This drug works by blocking the replication of the virus by blocking the action of the reverse transcriptase enzyme, and abacavir is taken with other antiviral drugs, such as: lamivudine (Lamivudine) and efavirenz, in order to avoid the development of resistant viruses to the drug.

Abacavir can be given as a primary treatment for AIDS patients, or for patients who have not responded to treatment and who have developed resistance to the action of other antivirals.

The most severe side effect of this drug is hypersensitivity, which is represented by the appearance of fever, breathing difficulties, rash and other symptoms. This side effect appears in 5-7% of patients who take the drug if they continue to take it or stop and then return to taking it again. This poses a threat to the patient's life.
Aprepitant is a drug that blocks the binding of a substance in the body called Substance P with its receptor, which helps prevent nausea and vomiting caused by chemotherapy. The drug is given with Ondansetron, Granisetron, or steroids.
Aprepitant is also used to prevent nausea and vomiting after surgery. Its effectiveness is to prevent nausea and vomiting, not to treat them after they occur, so it is often combined with other drugs that work by different mechanisms.
Side effects of aprepitant include: fatigue, nausea, constipation, diarrhea, loss of appetite, headache, and dizziness.

Eplerenone is given alone or with other medications to treat?high blood pressure?.
It also has another use, which is to reduce death rates and improve performance in people with congestive heart failure caused by a heart attack.
It works by blocking the aldosterone receptors in the body, and as a result there is a decrease in the reabsorption of sodium and water into the bloodstream.

Ebenastin is an antihistamine drug, used in the form of eye drops to treat the symptoms of??allergic??eyes, the drug works by stabilizing mast cells (mast cells) and thus preventing the secretion of histamine from them, and it treats allergies.
The drops contain a preservative that may be absorbed by soft contact lenses. Therefore, the lenses must be removed before using Ebenastin and wait at least 15 minutes after instillation, and then return the contact lenses to the eye.

Atazanavir is an anti-HIV medicine that belongs to the family of protease inhibitors and is used to treat people who have the virus that causes AIDS.
As with other antiviral drugs, to prevent resistance to the virus and to give the possibility of a stronger activity, atazanavir is given in combination with other antiviral drugs.
Common side effects of atazanavir include gastrointestinal disturbances such as nausea, vomiting,?abdominal pain?, diarrhea, and other effects such as numbness or mild stinging especially around the mouth, dizziness, headache, mood changes, and joint pain.

Etravirine is an antiviral drug used to treat patients who are infected with the human immunodeficiency virus (HIV) that causes?AIDS?.
Atravirine belongs to the family of non-nucleotide reverse transcriptase inhibitors (NNRTI) which inhibit viral replication.
It is taken with other antiviral drugs to avoid the development of resistant strains of the virus. It is often given to patients who have not responded to other antiviral treatments.
Most patients tolerate the drug well.

Etretinate is a drug chemically similar to?vitamin?A that is used to treat psoriasis in severe cases when other drugs are not feasible and under the supervision of a physician.
Etretinate affects the patient by reducing the amount of keratin protein that makes up the tough, outer layers of the skin, so itretin is considered successful in treating psoriasis.

Etodolac is a non-steroidal anti-inflammatory drug (NSAID) that reduces inflammation and pain in the body by inhibiting prostaglandins, which are chemicals released at the site of injury that cause pain and inflammation.
This inhibition is achieved by inhibiting the action of the cyclooxygenase enzymes (Cyclooxygenase - COX) responsible for the production of prostaglandins.
Etodolac is used to relieve mild to moderate pain and to treat symptoms of pain, swelling, and stiffness caused by??osteoarthritis?,?rheumatoid arthritis??, and arthritis in children.

Atorvastatin, like other medicines belonging to the family of statins, inhibits the action of an enzyme needed to produce cholesterol in the liver;?As a result, there is a decrease in the general level of cholesterol, triglycerides, and the level of harmful fats (LDL), which is one of the main factors in developing heart disease.
The drug also increases the level of beneficial fats (HDL), which leads to lowering the level of cholesterol in the blood and thus reduces the risk of heart disease. The drug is intended to treat a group of patients at high risk of heart disease or?stroke?.

Atovaquone and Proguanil are medicines used to treat malaria. These medicines work by separate mechanisms of action and share an effect on the genetic material (DNA) of the malaria-causing parasite, Plasmodium falciparum, to which each of these substances is resistant. On its own, the combination of these drugs leads to its destruction.?
The drug is effective in 98% of cases in reducing malaria, as this drug is good for children and adults, and the side effects are few compared to other drugs, they include digestive upset, abdominal pain, nausea, and headaches.

Atomoxetine is a drug used to treat attention deficit hyperactivity disorder (ADHD) and is part of a comprehensive treatment program to increase attention capacity and reduce impulsivity and hyperactivity in children and adults.
The drug belongs to a class of drugs called selective norepinephrine reuptake inhibitors (sNRIs), and it works by increasing levels of norepinephrine, a natural substance in the brain that is needed to control behavior

. This medicine is used to contribute to the treatment of problems of the heart and circulatory system.
Atenolol does not cure?heart disease,??but rather treats the symptoms. There may be a need to take atenolol regularly for a long time, perhaps even for life. Compared to other beta-blocker drugs, atenolol has a greater effect on the heart, in contrast, a small effect on other parts of the body.
Uses of atenolol
Atenolol is used to treat the following health problems:
Angina pectoris.
High blood pressure.
Irregular heartbeat (Arrhythmia).
Myocardial infraction.

l female hormone.
It is worth noting that estrogen and oestradiol are not found in a commercial drug alone, but rather placed with a type of progesterone.
Common uses of ethinyl oestradiol
Among the most important uses of synthetic estrogen are the following:
The contraceptive pill with synthetic progestin, which is the most common use.
For acne treatment

Monocerotene is a type of flavonoid and belongs to the family of bioflavonoids, a group of natural substances with a strong antioxidant effect.
Flavonoids are known to strengthen??blood vessels?and maintain their elasticity, so this drug is a vasodilator and anti-bleeding agent, and is used to treat varicose veins and chronic venous insufficiency.
But it seems that this drug has not yet been approved by the Food and Drug Administration and is under research and studies, so there is not much data available about it.

Adapalene is a drug that is chemically similar to vitamin A and used to treat?acne?.
It is supposed to remove the milky blockages stuck in the hair follicles.
The efficacy of this drug in removing milk blockages is similar to that of retinoic acid but in addition to this, it also has anti-inflammatory activity and causes milder skin irritation, and adapalene enhances the exfoliation process of dead skin cells.
The skin may dry out in the first weeks of treatment with adapalene,?redden?, and itch, but this situation improves with continued treatment, in addition to that, in the early stages of treatment, acne may worsen, and this is caused by the activity of the drug in more wounds It has a depth that was not noticed before, and this situation also disappears with continued treatment.
Adapalene causes sensitivity to sunlight, so you should avoid exposure to the sun and use protective creams before each exposure to the sun.

Adalimumab has been produced using genetic engineering technology and is similar to an antibody secreted by the body that binds with a protein called tumor necrosis factor alpha. This protein is produced properly in our body and has an important role in the process of inflammation and the activity of the immune system. The drug's binding to it prevents inflammation.
Common use of adalimumab
Adalimumab is used for inflammatory diseases in which the immune system is stimulated, such as:
Rheumatoid??arthritis.
Ulcerative colitis.
Ankylosing spondylitis??.
Crohn's disease.
psoriasis;
Psoriatic arthritis
Treatment for rheumatoid arthritis is usually given in combination with methotrexate, while treatment for Crohn's disease is given if previous treatments have failed.

Adefovir is an antiviral medicine used to treat chronic hepatitis B in adults and children who are at least 12 years old.
The mechanism of action of adefovir is to prevent viral replication by inhibiting the reverse transcriptase enzyme, which in turn reduces viral DNA synthesis, which leads to the inhibition of hepatitis B virus replication in the body.
But it is worth noting that adefovir will not cure hepatitis B and may not prevent its complications, such as: cirrhosis or liver cancer, and it may not prevent its spread to other people.

Adenosine is a natural substance found naturally in all cells of the body. It relaxes and widens blood vessels, and affects the electrical activity of the heart.
Adenosine is used to treat paroxysmal supraventricular tachycardia associated with Wolff-Parkinson-White syndrome (WPW), as it helps restore a normal heart rate.
Adenine is also used to diagnose cardiac function during a cardiac stress tes

Irbesartan is an antihypertensive drug with a unique mechanism of action that blocks the angiotensin 2 receptor, knowing that angiotensin II is a hormone that is present in our body and stimulates the contraction of blood vessels, which leads to the constriction of blood vessels in the body.
In people with type 2 diabetes who are at high risk of developing kidney disease, irbesartan preserves the kidneys and prevents protein from appearing in the urine (Proteinuria).
Unlike older medicines in the class of angiotensin converting enzyme inhibitors (ACE - angiotensin converting enzyme), arbesartan has a low incidence of side effects including cough, rash and changes in taste.

Ergotamine is a medicine used to treat headaches caused by??migraines?. Ergotamine generally constricts the blood vessels around the skull and is used only if pain-relieving medications such as Paracetamol have not sufficiently relieved the pain.
The drug is very successful if it is taken with the first signs of a migraine attack, while the effect of ergotamine is less if the drug is taken after the onset of the?migraine?attack .
The drug is more successful if it is taken with caffeine, and therefore there are preparations that combine these two compounds together.
Ergotamine causes reflex constriction of blood vessels, so it is not given to people with poor circulation.
Just as taking ergotamine frequently may seriously affect the blood supply to the hands and feet, it is forbidden to take ergotamine continuously to prevent migraine

Erlotinib is a biological drug that is used to treat certain types of cancer, such as lung cancer. It belongs to a group of anti-cancer drugs known to inhibit the activity of the enzyme tyrosine kinase, which is responsible for carrying out the chemical process that leads to cell growth and division.
This mechanism of action is selective, meaning that it targets cancerous cells only and not the body's normal cells.?Therefore, erlotinib does not cause the common side effects of chemotherapy, such as hair loss and bone marrow suppression.

Erythromycin is one of the safest and most widely used antibiotics.

Irinotecan is an anti-tumor drug called a topoisomerase I inhibitor. By blocking this enzyme, cancer cells will not divide, leading to their death.
Irinotecan is used to treat metastatic colon or rectal cancer that has not responded to prior chemotherapy with fluorouracil, and it is used alone or in combination with the drugs fluorouracil and leucovorin.
The irinotecan lipid complex is also used to treat??metastatic pancreatic??adenocarcinoma with fluorouracil and leucovorin.

Azithromycin is a new antibiotic belonging to the group of antibiotics called macrolides. These drugs disrupt the production of proteins in bacteria but not in humans.?

Azelastine is an antihistamine that prevents an?allergic reaction??by blocking the body's histamine receptors and inhibiting the release of histamine from mast cells.
Azelastine is marketed as a nasal spray and is used to treat symptoms related to hay fever and allergic rhinitis, such as runny and stuffy noses, sneezing, itching, and other nasal allergy symptoms.
Azelastine is also available as eye drops to treat itchy eyes associated? with allergic?conjunctivitis??.

There are several uses for acetazolamide, as it is used mainly to treat high blood pressure (glaucoma), to prevent and treat mountain sickness, and as a mild diuretic in cases of heart failure or edema arising from taking certain medications and as an additional treatment for seizures accompanied by coma (absence seizures).
Acetazolamide works by inhibiting the enzyme carbonic anhydrase, which produces bicarbonate and hydrogen ions from water and carbon dioxide. The enzyme lowers the concentration of bicarbonate and lowers intraocular pressure.
The drug increases the excretion of bicarbonate as well as other salts in the kidneys.

Estradiol is a synthetic estrogen with a potency similar to the natural female hormone.
Estramustine is an antimicrotubule agent that stops the growth and spread of cancer cells through its anti-androgen and microtubule effects, causing a decrease in testosterone and an increase in estrogen.
Estramustine is used for the palliative treatment of advanced or metastatic prostate cancer that has spread to other parts of the body. It limits, but does not cure, the cancer's spread.
Estramustine is contraindicated in patients with severe liver disease, serious cardiovascular disease, and thromboembolism.

Astemizole is an antihistamine used to treat?hay fever?, inflammatory sensitivity of the conjunctiva (the lining of the eyelid) and allergic rashes of the skin. Compared with other antihistamines, the hypnotic effect of astemizole is very limited.
Since there is a small possibility of adverse effects on the heart, the recommended daily dose should not be exceeded.?

Acebutolol is a medicine that belongs to the class of selective beta blockers. It works by widening blood vessels and slowing the heart rate to improve blood flow and lower blood pressure.
Acebutolol is used to treat high blood pressure and ventricular arrhythmias, and to lower blood pressure Acebutolol is often used in combination with other drugs, such as: thiazide diuretics.

Escitalopram is a drug indicated for the treatment?of depression?and anxiety disorders, and it belongs to the family of selective serotonin reuptake inhibitors (SSRIs), as it increases the level of serotonin in the brain.
Escitalopram works compared to citalopram in smaller doses and has a shorter effect within one to two weeks, and there is evidence that it has fewer side effects.
In?studies??comparing escitalopram to sertraline, escitalopram demonstrated similar efficacy to sertraline at doses smaller than 10 milligrams.

Acitretin is a drug chemically similar to vitamin A, which is used to treat skin conditions that do not respond to other treatments, such as: psoriasis, or other rare skin diseases associated with abnormal production of keratin (keratin). Keratin, which causes tough layers to form on the skin.
It is not permissible to donate blood during treatment with this medicine and even one year after the end of treatment, and you should refrain from continuous exposure to sunlight;?Because this medicine increases the sensitivity of the skin to sunlight.?This doubles the chances of getting burns.
The most common side effect that may appear with the use of this medicine is dryness of the skin and mucous membranes, especially on the face.

Acetylcysteine ??is a phlegm-laxative drug that helps eliminate pus in the respiratory tract and is frequently used in the treatment?of chronic bronchitis??, emphysema and cystic fibrosis.
Acetylcysteine ??is also used as an antidote in cases of??Paracetamol??poisoning, given intravenously or orally in successive doses.
This drug rarely causes severe side effects. However, the drug has an offending odor that can sometimes lead to nausea and vomiting, and its use can worsen shortness of breath in asthmatics.

Acyclovir is an antiviral medication used to treat herpes infections.

Ephedrine has been in use for more than fifty years, where it has been widely used as a bronchodilator because it relaxes the muscles surrounding the airway and thus relieves shortness of breath caused by asthma, bronchitis, and emphysema, but it can be replaced with newer drugs to treat these conditions .
If ephedrine is taken orally, it can irritate??the heart?and nervous system, causing anxiety and an increased heart rate.
Eflornitin is used today in the form of an ointment to slow and inhibit the speed of facial hair growth in women.
The use of eflornitin does not stop hair growth completely, but rather slows down the speed of its growth, and therefore it is necessary to continue removing?excess hair?by other means before applying the product.
Acarbose is an oral?diabetes??medication that, unlike other medications used to treat diabetes, stimulates the production and secretion of insulin by the pancreas, acarbose reduces the absorption of carbohydrates from the intestine and reduces postprandial hyperglycemia.
Acarbose is suitable for patients with type 2 diabetes, as it increases the effect of lowering blood sugar in patients who take drugs that stimulate the production of insulin from the pancreas, such as: Glibenclamide, because it works according to a different mechanism.

Ichthyl is a substance used to sterilize skin lesions.
Relieves itching and reduces the appearance of prominent lichenification among?chronic?eczema patients.
Side effects from ichthyol use are rare and include localized rash and itching.
This medicine consists of natural materials, so its efficacy and safety have not been studied by the Food and Drug Administration, so it should not be used without consulting a doctor.

Arsenic trioxide belongs to a class of drugs called antineoplastic agents. It slows or stops the growth of cancer cells by stimulating programmed cell death.
Arsenic trioxide is commonly used in combination with the drug tretinoin to treat APL in some patients as initial therapy, who have never responded to other types of chemotherapy, or who have recurring cancer after treatment.?
The use of arsenic trioxide can increase the risk of heart disorders that may be life-threatening, and this risk increases when it is used in combination with other medications.

Zinc oxide when applied topically forms an instant protective barrier to help heal and relieve pain caused by nappy rash and allergies. Recommended by pediatricians, it gives immediate relief to baby's delicate skin. It can also be used without a prescription.

Exemestane is a drug used to treat?breast cancer?. The drug blocks the aromatase enzyme that is involved in the final stage of estrogen production, causing damage to the growth of estrogen-dependent cancer cells.
Exemestane is intended to treat postmenopausal women only and has been approved for the treatment of breast cancer as a complementary therapy after 2-3 years of tamoxifen therapy.

Exenatide is a drug that mimics the functions of the hormone incretins, such as: glucagon-like peptide (GLP-1) in the body, and is intended for the treatment of patients with type 2 diabetes who are taking?metformin?, or other drugs of the sulphanylurea family ).
This drug doubles the secretion of insulin from the pancreas in proportion to the proportion of glucose in the blood. It also reduces the release of glucose from the liver by reducing its secretion, and slows down the duration of gastric emptying, as a result of which there is a decrease in appetite and a high feeling of satiety, which causes weight loss.
Atropine is an anticholinergic drug that inhibits the activity of acetylcholine in the parasympathetic nervous system.

Adrenaline, also called epinephrine, is the main neurotransmitter in the autonomic nervous system where adrenaline is formed in the center? of the?adrenal gland?.?

The use of aspirin has spread for more than 80 years, and it is a non-steroidal anti-inflammatory used to relieve pain, reduce?temperature?, and reduce?symptoms of arthritis?, and if used in a small amount, it contributes to preventing the formation of blood clots.
There are many uses for aspirin as a medicine?to treat colds?,?menstrual?pain, head pain as well as muscle and joint pain.
One of the most prominent side effects of aspirin is that it causes stomach irritation and bleeding, and it can also cause Reyes disease, a rare disease of the brain and liver that generally appears in children.

Conjugated estrogens are made from natural estrogens to relieve??menopausal?symptoms ?such as hot flashes and sweating as oral tablets are used.
These tablets are also used to treat and prevent symptoms of osteoporosis, which can occur in post-menopausal women, and is sometimes used as a palliative treatment for breast and prostate cancer.
When combined estrogen therapy is used as a hormonal replacement therapy, it must be taken periodically in combination with progesterone, usually in order to effect the hormonal changes that occur during the regular menstrual cycle.

Amantadine has been used since the 1960s as a preventive and curative drug against influenza type A (Influenza), and as a preventive drug, amantadine protects about 70% of patients who have not received influenza vaccination.
Amantadine is successful in relieving symptoms in people with influenza if taken within 48 hours of becoming ill.
A few years after it was started, amantadine was also found to be useful in relieving symptoms in patients with Parkinson's disease for a few weeks, while its effects wear off after a few months.
Sometimes this medicine is given together with another medicine called levodopa.

Insulin is a hormone produced by the pancreas and is vital in a number of metabolic processes, the best known of which is the control of blood sugar levels.
Insulin has been recognized as a drug since the 1920s, and is administered parenterally as an addition or alternative to natural insulin in the treatment of diabetes.
Insulin is the only successful treatment for juvenile-onset diabetes or??insulin?-dependent diabetes, and it is also given as a treatment for adult-onset diabetes.
It should be given while maintaining a well-balanced diet and closely monitored, and there may be a need to change doses in some cases of illness, vomiting, or changes in nutrition or levels of physical activity.
There is a wide variety of insulin drugs, the effect of which lasts for a short, medium or long period, sometimes several types of insulin are combined as directed by the specialist.
People undergoing insulin treatment should always carry a warning label indicating this, so that they can be given appropriate treatment if they lose consciousness in public.

Alprazolam belongs to a group of medicines known as benzodiazepines. These medicines are used to relieve anxiety, stress, relax muscles and aid sleep.
There are those who claim that alprazolam is particularly useful for treating cases of anxiety accompanied by depression. Doctors also prescribe alprazolam to treat cases of fear of open spaces known?as?agoraphobia??and other types of fear and anxiety attacks.
As with all other types of benzodiazepines, alprazolam may cause addiction if it is taken regularly and for continuous periods, and its effect may diminish over time.
Today there are other types of medicines that are used to treat different types of phobias.

Progesterone is a sex hormone that is secreted through the corpus luteum in the ovary after ovulation, which is responsible for thickening the uterine mucosa before pregnancy. This hormone is secreted in the last two weeks of the menstrual cycle.
In some cases, the activity of the particle may not be enough, which leads to a lack of progesterone necessary for pregnancy, so the body is supplied with progesterone in such cases to support the stability of the pregnancy and the dose is given through the vagina.
In addition to vaginal use, there are other oral uses related to the deficiency of this hormone, such as: premenstrual syndrome, amenorrhea, uterine bleeding, endometrial hyperplasia, and during menopause in combination with estrogen.
Because of the use of these multiple treatments, the risk of blood clots,?stroke?, and?heart attack?increases, and it can cause breast cancer as well, so the use of these treatments is prohibited for women at risk of infection, and the presence of a history of stroke, blood clots or cancerous tumors .

Alprostadil, or its scientific name, Prostaglandin E1) E1, is a substance with many advantages, most notably the following:
widening of blood vessels;
It helps involuntary muscles to relax.
Increases blood flow to the penis (male reproductive organ).
The main use of Alprostadil is to treat?erectile dysfunction?, where the drug is injected into the spongy tissue of the penis, and after a little training, most patients can inject Alprostadil themselves at home without any problems.
There are other uses for this drug, including the following:
Reducing side effects in babies born with congenital?heart?defects that require maintaining fetal blood flow.
Relieving symptoms caused by constricted blood vessels in patients with?Raynaud's disease??, an idiopathic vasculopathy.

Bismuth, present with subsalicylate or subcitrate, is a topical gastrointestinal soothing agent with weak antacid properties.
This medicine is used to relieve the symptoms of diarrhea,?heartburn?, and easy or moderate digestive disorders. It is also used in the treatment of stomach germs (?H. pylori?).

Penicillin is the first antibiotic discovered, and it has been in medical use since 1943.
It comes in two forms: Benzylpenicillin, usually given by injection, and phenoxymethylpenicillin, which is well absorbed when taken orally and is available as a tablet and syrup.

Albendazole is an anthelmintic medication that kills worms and prevents newly hatched larvae from growing or multiplying in the body.
It is used to treat various infections caused by worms, such as: neurocysticercosis caused by a pig tapeworm that affects muscles, brain, and eyes, and vesicular hydatidosis caused by a dog tapeworm that affects the liver, lung and abdominal lining.

Eletriptan is a medicine intended to treat acute?migraine headaches?of all kinds.
This medication is not intended to prevent headaches like newer migraine medications, such as: sumatriptan, zolmitriptan, rizatriptan, and naratriptan, but it does selectively act on a certain group of receptors. Serotonin: This process causes the blood vessels in the lining of the brain to constrict, thereby relieving migraine headaches.
The effectiveness of this drug and the appearance of its side effects depend on the concentration of the dose taken.

Testosterone is a male sex hormone that is produced naturally in the testes in men and in small amounts in the ovaries in women. This hormone stimulates bone and muscle growth in both men and women, and stimulates growth and puberty in men.
Testosterone deficiency may be caused by a disorder in the testicles or the pituitary gland, in which case synthetic or animal-derived testosterone can be given by injection or other methods.

Dopamine??is a sympathomimetic, a pharmacological form of a naturally occurring substance in the body that forms a neurotransmitter in the brain and sympathetic nervous system.
Dopamine is produced by levodopa and acts as a neurotransmitter by itself in the brain. It can also be converted in the body to noradrenaline.
It is worth noting that this drug is given only in hospitals, and under strict medical supervision.

Aldesleukin is a biological drug produced by genetic engineering technology, and it is similar to the protein Interleukin-2 (interleukin-2), which is naturally present in the body, and stimulates blood cells to resist inflammation, and the drug is also used to treat kidney and skin cancer.
Aldesleukin may cause abnormal heart rhythms and breathing disturbances;?Therefore, this medicine is contraindicated in patients with heart and lung diseases.
Its most common side effects include: fever, nausea, vomiting, headache, weight gain, low blood pressure, and diarrhea.
It's also been found that aldesleukin may also cause a life-threatening condition known as capillary leak syndrome, which is characterized by severe dizziness, fainting, irregular heartbeats, chest pain, difficulty breathing, changes in the amount of urine and mood swings.
Like other anti-cancer drugs, the drug interferes with the production of different blood cells in the bone marrow, which causes anemia.

Immunoglobulin contains immunoglobulins (Immunoglobulin - IG) that are given intravenously and therefore it is also called (Intravenous Immunoglobulin - IVIG).
It is a solution that contains human antibodies that give the body immunity within several days. Immunoglobulins are collected from the blood of donors after undergoing a preventive examination to prevent the transmission of viruses and diseases.
Immunoglobulins help reduce inflammation in patients with compromised immune systems who are more susceptible to infections such as CMV and HIV.
It is used to treat patients suffering from CLL - Chronic Lymphatic Leukemia, Multiple Sclerosis, Guillian Barre Syndrome and Kawasaki Disease, a rare pediatric heart disease.
Since there is a small possibility of the drug affecting the functioning of the kidneys, caution should be exercised when administering the drug to patients at risk of acute renal failure.

Glucagon is a synthetic drug similar to a natural hormone produced in the body. It is a glycogenolytic agent that raises blood sugar levels, so it is used for emergency treatment of severe low blood sugar in people with diabetes.
The system of action of glucagon is based on releasing glucose from the liver, which is stored in the form of glycogen, and excreting it into the blood.
Glucagon is also used to stop the stomach from moving during X-ray exams that are done to diagnose certain disorders of the stomach or intestines, as it relaxes the smooth muscles of the stomach and other digestive organs.


Vitamin??D is very necessary and vital in the metabolism process, especially calcium and phosphorous stores, as well as for the proper building process of bones, and sunlight is one of the main sources of vitamin D, however, in some cases, the need may arise to give medicines and supplements containing This vitamin, such as: Alfacalcidol
Alfacalcidol is used to treat the following patients and conditions:
Kidney disease.
Patients with?hypothyroidism?.
Preventing and treating some bone diseases resulting from vitamin D deficiency.?

Alfuzosin is a drug belonging to the family of selective alpha blockers, which is used to treat symptoms of benign prostatic hyperplasia, which include difficulty and pain in urination and frequent need to urinate.
Alpha receptors contribute to smooth muscle contraction, and are widely distributed in the prostate gland and the neck of the urinary bladder. Inhibition of the receptors by alfuzosin allows the muscles of the bladder and prostate to relax, which improves urine flow and relieves symptoms of the disease.
The symptoms of adenoma in the prostate gland are similar to the symptoms?of prostate cancer?(prostatic cancer), so before starting treatment with Alfuzosin, the presence of a malignant tumor in the gland must be excluded.

Quinine, which is extracted from the bark of the quinine tree, is the first drug to treat?malaria?. Quinine is not commonly used today because of its side effects, but it is sometimes used to treat malaria that does not respond to other safer treatments.
Quinine is sometimes taken by mouth in combination with other medications, given in low doses, to avoid painful nighttime cramps in the legs.
While quinine is used in high doses to treat malaria, it can cause ringing in the ears, headaches, nausea, hearing loss, and blurry vision. .

Lithium is a mood-stabilizing medication used to treat or control episodes of mania in people with bipolar disorder, or manic depression, that causes episodes of depression and mania.
Lithium also helps prevent or reduce the severity of manic episodes, whose symptoms include hyperactivity, rapid speech, poor judgment, poor sleep, aggression and anger.
It works by decreasing abnormal activity in the brain. Lithium affects the flow of sodium through nerve and muscle cells in the body, where sodium plays a role in states of excitement or mania.
In more difficult cases, lithium treatment can be started in a hospital and requires close monitoring because high levels of lithium in the blood can cause serious side effects.
It may take 2 - 3 weeks for lithium to have a positive effect, so there is a tendency for most cases to be given antipsychotic medication along with lithium for it to start working.

Melatonin?is a drug that mimics the activity of the natural sleep hormone (melatonin) in the brain and is used as a short-term treatment for primary insomnia with low sleep quality in patients 55 years of age and older.?As it seems, the drug's efficacy for the children of this generation stems from the low production of melatonin in the brain.?Compared to other alternatives, melatonin is not addictive, it allows the patient to sleep well for 8-12 hours and does not harm the degree of alertness the next day.?Most patients tolerate melatonin well, as common side effects include: head pain, back pain and weakness.
The nicotine in tobacco is largely responsible for the addiction to smoking, as nicotine is a stimulant that primarily affects the functioning of the sympathetic nervous system.
The nicotine in gum or patches can help people who are dealing with smoking addiction. The main side effects of nicotine are a feeling of bitterness in the mouth while chewing gum, local irritation of the skin while using the patches, and headaches

The term gout refers to a group of disorders in the metabolic process (Metabolism), which are represented by very high levels of uric acid in the blood. The complications of this phenomenon may include attacks of?arthritis?and kidney stones. The drug Allopurinol is used to prevent this type of attack. .
One of the reasons known today that may cause elevated levels of uric acid in the blood is anti-cancer treatments.
But since the effect of allopurinol is supposed to appear in the long term, it is not useful in relieving pain in an acute attack of?gout?, and in some cases may lead to an increase in symptoms when starting treatment, so it is followed to add colchicine during the first weeks of treatment. Gouty attack.
Unlike other types of drugs used against gout that lower the level of uric acid in the blood by increasing its excretion in the urine itself, allopurinol does not increase the risk of developing kidney stones, so it may be most suitable for people who suffer from kidney stones or for people who are prone to developing kidney stones. gravel in their kidneys.

Aliskiren is a medicine intended to treat high blood pressure. It belongs to a group of medicines called renin inhibitors, which help reduce high blood pressure.
Renin inhibitors eventually reduce the amount of angiotensin II that the body can produce. Angiotensin II causes blood vessels to constrict and narrow, which raises blood pressure, thus reducing its amount, leading to blood vessel relaxation and lower blood pressure.
It is known that?high blood pressure?increases the burden on the heart and arteries, and if it persists for a long time it can harm the blood vessels in the brain, heart and kidneys, which can cause stroke, congestive heart failure, kidney failure, and other complications.

Alendronate is a drug that blocks the osteoclast cells that digest bone, commonly used to treat?women?with osteoporosis in?menopause??and beyond, and patients with?Paget's disease?(inflammation of deforming bones) ).?
Alendronate is also used to prevent and treat osteoporosis caused by the use of glucocorticoids in menopausal women and men.
It is worth noting that in women who suffer from osteoporosis, treatment with alendronate should be combined with the addition of calcium and vitamin D, as needed, in addition to exercise. It is also desirable to consult a family doctor or a gynecologist regarding hormone replacement therapy.

Ambrisentan is an endothelin receptor antagonist. Endothelin is a natural substance that narrows blood vessels and prevents normal blood flow in pulmonary arterial hypertension (PAH).
Ambrisentan's mechanism of action is to block the activity of endothelin, thereby lowering blood pressure in the lungs, helping the heart to pump blood more efficiently.
Ambrisentan, used alone or in combination with tadalafil, to treat pulmonary arterial hypertension in adults may improve exercise capacity and slow the progression of symptoms.

Ampicillin is a penicillin antibiotic that has been known since 1966 and has been used to treat a number of infections. In some cases, ampicillin can be used to treat gastrointestinal infections caused by?Salmonella?or Shigella bacteria?,?but these bacteria have acquired resistance to the drug over time.
It can also happen with any other type of penicillin antibiotic. Also, ampicillin may cause a severe allergic reaction that causes fever, swelling of the mouth and tongue, itching and shortness of breath.

Emtricitabine is an antiviral medicine used to treat people who are infected with the human immunodeficiency virus (HIV) that causes acquired immunodeficiency syndrome or AIDS. It is used in combination with other antiviral medicines.
This drug is a nucleoside reverse transcriptase inhibitor, and by this mechanism it works to prevent the replication of the virus inside the body.
It is worth noting that emtricitabine does not cure HIV, but it does reduce the chances of developing AIDS and associated diseases, such as infection and cancer.
Amphotericin B is a medicine used to treat life-threatening infections caused by fungi.
Amphotericin B is used to treat infections caused by certain parasites, such as Leishmania, which affects the skin tissues, and inflammation of the brain and brain membranes caused by Amoeba. The mechanism of the drug's effectiveness is to kill fungi and prevent their reproduction.
Amphotericin is mainly administered by intravenous injection as a sulfate or lipid-containing formulation, or as a liposomal formulation. The goal of developing these drug formulations is to reduce their toxicity.
Oral amphotericin B preparations are available and are used in the treatment of?candidiasis?of the oral cavity.
The toxicity of intravenous amphotericin is that it may cause kidney and liver damage, and abnormal heart rhythms.
Imipramine is a medicine that belongs to a class of antidepressants called tricyclic antidepressants.
Imipramine improves functionality, stimulates physical activity, increases appetite, and restores the patient's interest in daily life.
Common uses of imipramine
Imipramine is primarily used to treat the following:
depression?.
Various psychological disorders, such as: anxiety, panic attacks and panic attacks.
Nocturnal enuresis??in children, or some other urine leakage.
Imipramine is less alert and hypnotic than other tricyclic antidepressants, however it should be noted that imipramine can exacerbate sleep disturbances if taken in the evening.
Amoxicillin is a penicillin-type antibiotic used to treat certain diseases caused by certain bacteria sensitive to the drug.
Clavulanic acid is a substance that inhibits the beta lactase enzyme. These enzymes break down the antibiotic before they can kill the bacteria.
Clavulanic acid is added to prevent the breakdown of amoxicillin by beta-lactase enzymes in bacterial bodies, so the combination of amoxicillin with clavulanic acid is effective in treating ear infections, nose infections, and infections??sinus??infections, lung infections, skin infections, and urinary tract infections.
Amoxycillin is a penicillin antibiotic that is used to treat a range of bacterial infections, but it is very successful in treating the following conditions:
Infection of the ear, nose and throat.
Infection of the respiratory tract.
Urinary cystitis.
Mild?gonorrhea .
Some types of infections in the skin and in soft tissues.
Amoxicillin is well absorbed into the body if taken orally and starts to work quickly and effectively. As with other penicillin medicines, the most common side effect of amoxicillin is a rash that appears in the form of spots on the skin.
Amoxicillin may also provoke a more severe allergic reaction represented by other symptoms, including high temperature, swelling of the mouth and tongue, itching and shortness of breath.
Unfortunately, we have recently witnessed an increase in the number of types of bacteria that become resistant to amoxicillin, so if there is no decrease in the severity of the symptoms, then you should consult a doctor who may take a sample from the affected area and decide to switch the type of antibiotic.?
Amlodipine is a vasodilator drug belonging to the family of calcium channel blockers, used to treat patients with??high blood pressure and??angina pectoris. Because it belongs to the family of calcium blockers, amlodipine affects the signal transduction process in the heart muscle and in the blood vessels.
Like other calcium blockers, amlodipine may cause a very severe drop in blood pressure, although this is a rare phenomenon. Common side effects include fluid accumulation, edema, and headache.
Amiloride is a potassium-sparing diuretic that is given in combination with another type of diuretic in the same tablet for the treatment of patients suffering from?hypertension??,?congestive heart failure??and other edematous conditions.
Since amiloride leads to the retention of potassium ions in the body, caution should be exercised when administering it to patients who are taking other potassium-sparing medicines or to patients with kidney disease or diabetes.
One of the main advantages of amiloride in the treatment of high blood pressure is its cheap price.
Amikacin is an antibiotic belonging to the aminoglycoside family. Amikacin is used to treat a wide range of bacterial infections, including: respiratory tract infections, skin infections, urinary tract infections, blood infections, and bone infections.
The mechanism of action of amikacin is to inhibit the process of multiplication and multiplication of bacteria, especially Gram-negative bacteria such as those that cause?urinary tract infections?, and a portion of Gram-positive bacteria such as those that cause?endocarditis?.
Amikacin is used in the second-line treatment of infections that have shown resistance to other aminoglycoside antibiotics, such as: gentamicin and tobramycin.
Imiglucerase is given by intravenous infusion, and is used as an alternative treatment in patients with Gaucher's disease who have one of the following symptoms: anemia, thrombocytopenia, bone disease, and an enlarged spleen.
Treatment with amyglucerase helps to break down and break down the stored fat, so that the functioning of the tissues and organs in which the fat has accumulated becomes healthy and prevents further progression of the disease.
Amisulpride is a drug belonging to the family of atypical antipsychotics, and its system of action depends on selectively blocking the activity of certain dopamine receptors.
Amisulpride is primarily used to treat acute or chronic schizophrenia in patients who present with symptoms: delusions, hallucinations, absurd thoughts, decreased motivation and social abilities, and even psychological state.
It may also be used in the prevention and treatment of nausea and vomiting after surgery in adult
Amitriptyline belongs to a group of antidepressants called tricyclic antidepressants and is primarily used to treat depression.

Amitriptyline increases performance, stimulates physical activity, improves appetite, and restores interest in daily activities.
Because amitriptyline disrupts the nervous system more than other TCAs, it works when depression is accompanied by fear and insomnia.
When taken at night, amitriptyline helps sleep and eliminates the need for hypnotic drugs. If taken in excess, amitriptyline can cause a deep coma and a serious irregular heartbeat.
Amitriptyline is also given to treat the following conditions:
Urinary incontinence?.
Neuropathic pain.
Fibromyalgia.
Attention Deficit Hyperactivity Disorder?(ADHD).
Anxiety disorders.
Aminophylline is a bronchodilator belonging to the methylxanthine family that is used to relieve symptoms of asthma or to prevent asthma and to treat non-chronic bronchospasms associated with chronic inflammation of the bronchi.
Aminophylline is practically a mixture of theophylline and ethylenediamine, since under normal physiological conditions in the body there is a secretion of theophylline, which relieves the shortness of breath and the wheezing that characterizes these respiratory diseases.
Most of the side effects caused by aminophylline include: nervousness, headache, rapid heartbeat, and sleep disturbances, which vary according to the level of this drug in the blood;?Therefore there is a need to monitor and monitor the level of this medicine in the blood on a regular basis.
Amiodarone began to be used in the fifties of the last century, but only in recent years has its use spread as a treatment for a wide range of heart rhythm disorders (Arrhythmia). Amiodarone works by slowing nerve impulses in the heart muscle.
Amiodarone is given to prevent recurring atrial??fibrillation??, auricular fibrillation and ventricular fibrillation, and to treat?ventricular?tachycardia. It is also used to treat Wolff-Parkinson-White syndrome (WPW).
Amiodarone is usually treated as a last resort if other medications do not work, due to the severe side effects it causes, especially with continued use.
Anastrozole blocks the enzyme aromatase, which is involved in the last stage of estrogen production, and anastrozole is a drug intended for the treatment of breast cancer in postmenopausal women only.
Certain types of?breast cancer are?related to estrogen, so blocking estrogen production with anastrozole prevents tumor development and growth.
Anagrelide is used to treat a disease called essential thrombocythemia (ET), in which the level of cells responsible for the production of platelets in the bone marrow increases.
Anagrelide prevents these cells from multiplying, causing a low platelet count and reducing the risk of blood clots that can block blood vessels and cause death.
The medicine can cause side effects in the heart in 1% - 5% of patients. These effects include: heart failure, arrhythmias, angina pectoris, high blood pressure, and heart attack;?Therefore, it should be used with caution in patients with heart disease and only when the potential benefit outweighs the risks.
One of the common treatments for epilepsy includes the combination of levodopa with carbidopa or benserazide. Levodopa breaks down in the body into dopamine, the same substance that, due to its deficiency or its presence in small quantities in the brain, causes epilepsy. Carbidopa or benserazide increases the effect of levodopa in the brain, enabling the drug to be taken in smaller doses while reducing the side effects of the drug.
The problem with this treatment lies in the disappearance of the effectiveness of the dose before taking the next dose, and this happens more with the progression of the disease, as the entacapone drug prolongs the effect of treatment with previous medicines.
Entacapone works by inhibiting the enzyme O-methyl-catechol transporter (COMT) during the presence of the aforementioned drugs in the body, as this enzyme is the main responsible for the breakdown of levodopa. Therefore, inhibiting the action of this enzyme enables greater amounts of levodopa to reach the brain and be transformed There to dopamine.
Entacapone is only used when combined with these medications, as it does not affect the symptoms of Parkinson's disease when taken alone.
Antipyrine, also called phenazone, is a pain reliever that is generally given with a local anesthetic, such as tetracaine, amethocaine, or benzocaine as ear drops.
Ear drops are often made on the basis of glycerine, and glycerine softens the?wax?in the ear, allows the maximum amount of time to stay between the active substances and the ear tissue, absorbs moisture from the tissues, thus creating an undesirable environment for microorganisms and reduces inflammation.
The common causes of?earache are infections of the middle?or outer ear, which are caused by bacteria or fungi, such as the development of a cold or inflammation of the upper respiratory tracts, and it must be emphasized that the drops are not intended to treat the infection itself, and therefore requires a separate antibiotic treatment.

Intecavir is an antiviral medication that is used to treat??hepatitis??B conditions in adults and children over 2 years old.
The mechanism of action of entecavir depends on impeding the replication of the virus in the body by inhibiting the reverse transcriptase enzyme, which leads to the elimination of the virus as quickly as possible. Entecavir is characterized by the low rate of resistance that the virus can develop against it.
After you have finished taking it, intecavir may cause an exacerbation of hepatitis;?Therefore, patients who stop taking this drug must be kept under close medical monitoring of liver function, and kidney function damage may also occur in patients at previous risk of kidney damage.

Indapamide is a medicine from the sulphonamide family, used to treat?high blood pressure and??edema caused by heart failure. This medicine works in a similar way to medicines of the thiazides family of diuretics, but it is preferable to thiazides because it does not accumulate in the body during renal impairment.
Common side effects of the drug include: back pain, diarrhea, dizziness when moving from a lying to standing position, headaches, and stomach irritation

Indomethacin is a nonsteroidal anti-inflammatory drug that relieves pain, relieving stiffness and inflammation.

Indinavir?is an anti-HIV medicine that?belongs to the family of protease inhibitors.
The virus is able to resist the drug after a short period, so this drug is given in combination with other antiviral drugs

Infliximab was produced using genetic engineering technology. It is similar to an antibody secreted by the body that binds with a protein called tumor necrosis factor alpha. Immunity, the drug's binding to it helps prevent inflammation.

Auranofin was first introduced in 1987 as an orally administered drug for the treatment?of rheumatoid?arthritis.
Auranofin can slow the progression of the disease, however, it is a drug with a high toxicity, and most doctors prefer to prescribe other treatments as long as the arthritis is in a stable condition, but when the first signs of abnormalities in the joint appear that indicate a rapid deterioration in the course of the disease, then auranofin treatment can be started.

Orphenadrine is an anticholinergic drug that is primarily used to relax muscles and was used in the past to treat?Parkinson's disease.??Although it is less effective than other medications used to treat Parkinson's disease, its side effects are less severe.
Orphenadrine has a great muscle relaxing effect by blocking the nerve pathways responsible for stiffness and muscle spasm, so it is used to relieve?muscle spasms?caused by muscle damage.

Orlistat is a drug intended to treat obesity in addition to a low-calorie diet. This drug is suitable for people with a body mass index (BMI) of 30 or more, who are at risk of risk factors such as??high blood pressure??and diabetes, and who have high blood lipids.
Orlistat inhibits the action of lipases, an enzyme that helps digest fats in the intestines, thus preventing the absorption of fats in the body, as the absorption of fats from food is inhibited by at least 30%.

Oseltamivir is an antiviral that is used to kill the influenza virus (Influenza) of both types: influenza A and influenza B.
The medicine is used to treat?flu??symptoms if they begin within two days, or to prevent infection.

Ofloxacin is a quinolone antibiotic that is used to treat various infections caused by bacteria sensitive to this antibiotic, and is specifically used to treat infections in the urinary tract, respiratory tract and some infections in the intestine.
Ofloxacin is distinguished from other quinolones by its high bioavailability when taken orally, and its bioavailability means that a high percentage of the drug reaches the blood plasma.
The main side effects of ofloxacin are: nausea, headache, and rarely hallucinations. When ofloxacin is prescribed to patients with impaired renal function, the dose should be reduced in accordance with the level of renal performance.

Octreotide is one of the drugs that is used to treat many conditions, such as: cell hyperplasia, and it is??one of the drugs that is similar in action to somatostatin, which is one of the natural hormones responsible for the secretion??of growth hormone??(GH), in addition, it prevents Secretion of some substances from the hormonal glands of the digestive system, such as: serotonin, insulin and glucagon.
Octreotide is used to treat many conditions, such as??acromegaly??and some carcinoid tumors. It can also be used to prevent complications that may result after pancreatic surgery, and to relieve diarrhea associated with some cancerous tumors.
The treatment may cause many side effects, such as: digestive disturbances,?abdominal pain?, nausea and vomiting, and disturbance of blood sugar levels.

Oxazepam, which has been in use since 1965, belongs to a group of medicines called benzodiazepines. These drugs help relieve tension and anger, relax muscles, and help induce sleep.
Oxazepam is used to treat?anxiety??, fear, and insomnia, although the effect of oxazepam does not start quickly, but its effect lasts for a relatively long time, so oxazepam is more suitable for treating early awakening than for difficulty falling asleep.
Oxazepam accumulates in the body to a lesser extent than other similar drugs, so it is especially suitable for people with impaired liver function.
Benzodiazepines are recommended for the treatment of fear and anxiety only in acute and transient attacks and only on the recommendation of a doctor, but in the case of persistent fear or excessive anxiety it is not recommended to use it, but doctors usually recommend the use of special drugs from the family of selective serotonin reuptake inhibitors (SSRI's - Selective Serotonin Reuptake Inhibitor). .

Oxaliplatin is an anticancer used in combination with fluorouracil and leucovorin to treat patients with grade 3 colon cancer after an operation to remove the precancerous tumor, or in patients with advanced bowel and rectal cancer.
Oxaliplatin binds to the genetic material in the cell and damages it, thus preventing the growth and division of cancer cells.
Like other anti-cancer drugs, this drug's mechanism of action may negatively affect healthy cells, impairing the production of various blood cells in the bone marrow, leading to anemia.

Oxcarbazepine, chemically similar to carbamazepine, is an anticonvulsant drug suitable for the treatment of partial?seizures?. Leukopenia).
This medicine does not require frequent tests and measurements of its concentration in the blood, as it interacts slightly with other medicines.
Oxcarbazepine is used alone as a first-line treatment, or as an addition to other medications, or as an alternative treatment in patients who cannot tolerate other medications, or to treat pain caused by damage to the nerves of the skull, such as: Trigeminal neuralgia.

Oxolamine is a drug used in some countries as a cough suppressant. It has anti-inflammatory activity for the treatment of pharyngitis and inflammation of the respiratory tract associated with dry cough, such as:??bronchitis?, bronchitis ?, bronchiectasis and whooping cough.
As with other cough suppressants, oxolamine should not be used to treat a cough that produces phlegm or a cough of unknown cause.
It is worth noting that the use of this drug is not licensed in the United States of America.

Oxomemazine belongs to a group of medicines called phenothiazines, which are sedative and antihistamines. Oxomemazine is actually used as an antihistamine to treat allergies and to relieve itching in a variety of skin conditions.
Oxomimazine is a medicine used to prepare a remedy for the symptoms of coughs and colds. It is an anti-cough syrup and an aid in the excretion of phlegm. It is also used as an antihistamine to treat allergies and to relieve itching in a number of skin diseases.

Oxytetracycline is an antibiotic belonging to the tetracycline group, and it is used to treat several types of infections, such as: infections that affect the skin, respiratory tract, urinary tract, ears and eyes, as it works by inhibiting the process of manufacturing proteins necessary for bacterial growth and reproduction.
Use oxytetracycline as an alternative if you are allergic to penicillin or macrolides.
Oxytetracycline, similar to other tetracyclines, may cause staining in developing teeth and bone growth disturbances.?Therefore, it is not recommended for use in children and pregnant women.
Oxytetracycline is commonly found in pharmaceutical preparations in combination with other antibiotics called polymyxin B sulphate, a family of polymyxins. Oxytetracycline is also present in a wide range of veterinary preparations.
The side effects in topical use are rare, but if it is used orally, it may have effects in the digestive system such as: nausea, vomiting, and diarrhea. In addition, the drug may cause an increased sensitivity to light

Oxycodone is a narcotic pain reliever of the opiate family. Oxycodone is used to treat moderate to severe pain, such as: pain caused by surgery, wounds, or chronic diseases, such as cancer.
Like other pain relievers of this family, the intake of this drug is very limited, because it can cause a feeling of pleasure and euphoria that may lead to its abuse and addiction.
But when oxycodone is taken under medical supervision to treat severe pain for a short period of time, the potential for addiction is virtually non-existent.

Oxymetazoline is a topical drug that relieves nasal congestion. The goal of these preparations is to relieve congestion in the nose due to colds, sinusitis, or??Hay Fever. Oxymetazoline may also be used to treat simple red and itchy eyes?.
Oxymetazoline has adrenergic properties as it activates the alpha-adrenergic receptor, which leads to the contraction of the capillaries in the nose and sinuses, and the reduction of mucous secretions.

Olanzapine is an antipsychotic drug that is used to treat?schizophrenia??and does not lead to side effects in the blood such as causing damage to white blood cells, and therefore it does not require continuous follow-up and monitoring and a complete blood count (CBC) constantly.
This medicine causes fewer side effects related to the ability to move, and weight gain appears in a small number of patients.
On the other hand, it can cause a sharp and excessive drop in blood pressure when moving from a lying position to a standing position, especially in the first times that the drug is taken, so it is recommended to rest after taking the drug, especially in the first days of starting it.


Olmesartan is a drug of the class of angiotensin II receptor antagonists (ARBs). Angiotensin II is a substance in the body that stimulates the contraction of blood vessels, and by blocking its activity, blood vessels dilate, thereby lowering blood pressure.
?
Olmesartan is used alone or in combination with other medications to treat high blood pressure in adults and children 6 years of age and older.
As with other medicines of its family, a higher anti-hypertensive effect can be obtained when we add to olmesartan low-dose diuretics, such as: Hydrochlorothiazide.

Olopatadine is an antihistamine in the form of eye drops, used to temporarily prevent irritation in the eyes that may occur due to allergic conjunctivitis. The function of this drug is to prevent the release of histamine that causes an allergic reaction and prevents its effective action in the formation of inflammation.
This preparation contains a preservative that can be absorbed by contact lenses. Therefore, you must remove the lenses before using this preparation and wait at least 15 minutes before putting the medication in the eye. In the event of redness in the eyes, contact lenses are strictly prohibited.

Omalizumab is a newer drug given to treat severe asthma that presents as daily attacks, attacks at night, or severe attacks that occur several times a week, or for people whose asthma symptoms cannot be controlled by treatment with inhaled corticosteroids.
Omalizumab is generally given by subcutaneous injection into the arm once every two to four weeks. The drug is also given with corticosteroids. It is not intended to treat an attack immediately, as several weeks may pass from starting treatment until you see an improvement in asthma symptoms.

Omeprazole is used to treat cases in which excessive amounts of acid are secreted in the stomach. It inhibits the action of some enzymes responsible for acid secretion, thus preventing acid production.
Omega-3 acid ethyl esters is one of the drugs that is used to lower levels of triglycerides in the blood?,?and also contributes to the prevention of diseases caused by blockage of blood vessels, such as myocardial infarction and stroke.
It is necessary to know that omega-3 acid ethyl esters is only prescribed under the supervision of a doctor, depending on the patient's health condition and the extent of his response to treatment.
The benefits that this treatment may give must be weighed against the potential risks it may cause, and you must stick to taking the treatment even if you feel well, as high triglycerides do not cause any symptoms.

Ondansetron is well-tolerated by most patients. It blocks serotonin receptors and is used to prevent nausea and vomiting caused by chemotherapy, radiotherapy, and after surgery.
Serotonin is released in the body as a result of chemotherapy and affects the vomiting center in the brain. Ondansetron binds to the serotonin receptor and blocks its action, preventing nausea and vomiting.
Ondansetron is usually given before chemotherapy by injection while it is taken after chemotherapy with tablets for several more days. Dexamethasone is sometimes added to increase the effectiveness of ondansetron.

Oestriol is??one of the types of female hormones that are naturally manufactured in the body, especially during pregnancy.?Therefore, its concentrations are continuously measured to ensure the general health of the fetus.
Oestriol is used as a hormone replacement therapy (HRT - Hormone Replacement Therapy) in cases of vaginal atrophy caused by low estrogen levels in the body during?menopause?. It may also be used before and after vaginal operations.
It is important to know that the treatment is contraindicated in cases of some diseases, such as:? breast?cancer??, ovarian cancer, endometrial carcinoma, as well as severe liver diseases.

Ipratropium bromide, which was introduced as a bronchodilator in 1975, is used to treat obstructive pulmonary diseases, especially in patients suffering from?chronic bronchitis?.
Ipratropium bromide, a derivative of tropine, inhibits the effect of acetylcholine on the bronchi, which leads to their expansion and facilitates breathing. Ipratropium bromide is given by inhalation only, so no serious side effects are expected in general.
Also, a nasal spray has recently been started to treat?allergic?rhinitis, and it is worth noting that due to the slow effect of ipratropium bromide, it is not recommended to use it when severe asthma attacks occur.

Ibuprofen is a nonsteroidal anti-inflammatory drug.

Ipoietin alfa is genetically modified to be produced in the body as erythropoietin, which is the main hormone responsible for the production of red blood cells in the body.
Ipoetin alfa is used to treat anemia caused by many conditions, such as: patients with??chronic kidney failure?, AIDS patients treated with zidovudine, cancer patients receiving chemotherapy, and patients who need an automatic blood transfusion before surgery.
Ipoietin alfa may be used less commonly to treat anemia in premature infants, as well as in patients with chronic infections, such as:??arthritis?, and patients with hepatitis C.
The use of epoetin alfa may cause many side effects, such as: blood clots, red blood (Polycythemia), and sometimes the body may make some antibodies against erythropoietin, which causes an allergic reaction.
In most cases, some tests are recommended during treatment, such as: A blood count (CBC) including platelet count, blood pressure levels and hemoglobin levels.

Etanercept?is a drug that is produced by genetic engineering technology, thus it is similar to the antibody produced by the human body.
Its mechanism of action depends on binding to a protein in the body called Tumor Necrosis Factor - alpha, as it plays an important role in activating the immune system and regulating inflammatory processes in the body.
This drug is used in inflammatory diseases that affect the immune system, such as: rheumatoid arthritis, ankylosing spondylitis, psoriatic arthritis, and psoriasis. aged 4 to 17 years with juvenile rheumatoid arthritis.
It is important to know that this treatment does not cure these diseases, but rather contributes to reducing the symptoms caused by inflammation, thus hindering the progression of the disease and reducing the damage caused by it.
Etanercept reduces the body's immunity, so it makes it more susceptible to opportunistic diseases such as tuberculosis, and therefore the patient's health condition should be monitored while receiving treatment with this drug.?

Itraconazole is an antifungal medication that inhibits the building process of the fungal cell wall.

Etoposide is a podophyllotoxin derivative, an anticancer drug that works by blocking the transcription of the genetic material of cancer cells, thereby inhibiting their division and death.
Etoposide is used with other anticancer medicines to treat small cell lung cancer (SCLC) and testicular cancer that has not responded to other treatments

Etoricoxib belongs to a group of nonsteroidal anti-inflammatory drugs (NSAIDs) and is a newer selective cyclooxygenase-2 inhibitor.
Etoricoxib is used to treat and relieve the pain and symptoms of inflammatory disorders caused by??rheumatoid arthritis?,?osteoarthritis?, ankylosing spondylitis, gout, acute and chronic pain, and dental surgery.
Unlike older version NSAIDs, this medication appears to cause fewer gastrointestinal side effects.
People who are allergic to other non-steroidal anti-inflammatory drugs (NSAIDs) and aspirin should not take this drug, and people with asthma should be careful not to use etoricoxib.

Ethosuximide is an anticonvulsant medication that is used to prevent epileptic seizures, often for a limited period of time no longer than a few years.
As with most drugs that affect the central nervous system, this drug can also cause dizziness, headache, and drowsiness, and the patient may have suicidal thoughts.?Therefore, a doctor should be consulted immediately in the event of symptoms such as: depressed mood, anxiety and other behavioral changes.
Ethosuximide also suppresses the production of various blood cells in the bone marrow, which leads to severe anemia, infections and unusual bleeding.

Isotretinoin is a derivative of vitamin A chemically, used in the?treatment of acne?K, it is taken to treat severe cases of pimples or severe acne that does not respond to other treatments.
Isothipendil is a first-generation antihistamine used to treat allergy symptoms and relieve?itching?by blocking histamine 1 (H1) receptors.
The drug is often marketed as a gel and is used to temporarily relieve itching caused by mild skin disorders such as: stings, irritation, sunburn, and allergic dermatitis.
It is not recommended to use Isothipendil on a wide surface of the skin and on injured or inflamed skin.
This drug is still being tested

Isosorbide 5 Mononitrate is an effective derivative of Isosorbide dinitrate, which is used to treat?angina??and heart failure.
Compared with?isosorbide dinitrate??, the digestive system absorbs isosorbide mononitrate better, and its effectiveness and its effect lasts for a longer period, thus eliminating the patient from taking more than two doses per day.

Isosorbide Dinitrate belongs to the family of vasodilators known as nitrates, which also includes glyceryl trinitrate.
Isoconazole is an antifungal drug commonly used to treat infections caused by?fungi?and yeasts. This drug is successful and effective in treating fungal skin infections, vaginal yeast infections or vaginal candidiasis.
Side effects of isoconazole are rare, however some patients may feel burning and irritation in the affected area of ??the skin.
Isoniazid is a medicine used to treat?tuberculosis??and to prevent tuberculosis in people at risk.
Indications for use of isoniazid, depending on age
The reason for dispensing isoniazid medication varies according to the age group, as follows:
1. Persons over 35 years old
Azoniazid is recommended for people over the age of 35 who are at risk for tuberculosis, such as:
People with??weak?immunity .
Patients receiving treatment with corticosteroids.
Persons suspected of having the disease.
2. Persons under 35 years old
Ezetimibe is a new drug for the treatment of high blood cholesterol level. Ezetimibe is given alone or in combination with other drugs from the family of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA reductase) inhibitors.
In contrast to other drugs, ezetimibe does not affect the absorption of fat-soluble vitamins, and ezetimibe has been found to be a well-tolerated drug in patients.
When ezetimibe was given with a statin, the side effects were similar to those that appear when taking a statin, except for a sharp rise in the level of liver enzymes in the blood, which may be an indication of a disorder in the work of the liver. With time or after stopping treatment.
Efavirenz is a medicine used to treat people who are infected with the human?immunodeficiency virus?(HIV) that causes AIDS.
This drug belongs to a group of drugs that inhibit the reverse transcriptase enzyme, vital for the development of the virus in cells of the immune system.
This medicine is given in combination with other additional medicines and should not be taken alone in any case.
Efalizumab is a drug intended to treat moderate to severe adult psoriasis, an autoimmune disease that causes abnormally fast skin cells to form silvery scaly patches of skin.
Psoriasis occurs as a result of activation of the immune system, especially T lymphocytes, which must attach to other cells through receptors on their surface to be activated.
Evalizumab is a synthetic monoclonal antibody that blocks one of these receptors on lymphocytes and prevents their adhesion, thus inhibiting the activation of lymphocytes responsible for psoriasis.
Everolimus is a derivative of Sirolimus, and it belongs to a class of drugs called kinase inhibitors. This drug reduces blood flow to cancer cells and prevents their growth and spread. It also prevents rejection of a transplanted organ by decreasing the activity of the immune system.
Common uses of everolimus
Everolimus is commonly used to treat the following conditions:
Prevent rejection of a transplant after a kidney or liver transplant when used with cyclosporine, corticosteroids, and other medications.
Treating some types of pancreatic cancer, stomach cancer, bowel cancer, or metastatic or advanced lung cancer.
Treatment of advanced renal cell carcinoma (RCC) that has not responded to other medications.
Treating some types of advanced breast cancer that has not responded to treatment with at least another drug.
Treating kidney tumors in people with tuberous sclerosis complex, an inherited condition that causes tumors to grow in many organs.
Treating certain types of seizures in adults and children 2 years of age and older with tuberous sclerosis complex when used together with other medications.
Treatment of subependymal giant cell astrocytoma in adults and children 1 year of age and older with complex tuberous sclerosis.
Econazole is an antifungal drug that is used to treat several conditions caused by fungal infections. Econazole is primarily used to treat vaginal yeast infection, and it is also used to treat foot fungus, and fungal infections in?children?caused by wet diapers.
The affected area should be thoroughly washed and dried before applying the medicine.
When there is strong local inflammation associated with a fungal infection, an ointment containing an anti-inflammatory and econazole can be used together.
Iloprost is a synthetic analogue of prostacyclin which is a molecule responsible for the dilation of arteries, including the pulmonary arteries.
Iloprost is used by inhalation to treat pulmonary arterial hypertension (PAH) in adults. It relieves symptoms temporarily and may improve exercise capacity.

Imatinib is used to treat chronic myeloid leukemia (CML) and to treat connective tissue cancer of the gastrointestinal tract.
Imatinib suppresses the production of various blood cells in the bone marrow, which causes anemia and increases the risk of infections. The most common side effects that have been observed as a result of using this drug include: nausea, vomiting, muscle cramps, edema, and fluid buildup, which leads to: Complications such as: pulmonary edema, fluid leakage into the membrane that covers the lungs and the membrane that covers the heart.
Imiquimod is a cream used for the topical external treatment of warts caused by HPV in the genital and anal area in adults.
It should not be applied to open wounds or irritated skin or to a place before it has been cured by other medicinal or surgical treatment, and exposure to sunlight should be avoided as much as possible during the course of treatment with the medicine.
When treating genital or anal warts, sexual contact should be avoided as long as the cream is on the skin.
Enalapril belongs to a group of medicines that widen the blood vessels called angiotensin converting enzyme inhibitors (ACEIs) that are given to treat?high blood pressure??and congestive heart failure. In many cases, enalapril is given with another medicine in order to increase its effect.
Taking the first dose of enalapril can cause a sudden drop in blood pressure, so it is recommended that the patient lie down when receiving the first dose for a period of two to three hours.
The most common side effects are dizziness and headache, but they quickly disappear with the continuation of treatment. A rash may appear, but it also quickly disappears with stopping the medication, and in some cases the rash disappears automatically even with the continued use of the medication.
Enfuvirtide is an antiviral medicine used to treat adults and children over 6 years of age who are carriers of the acquired immunodeficiency virus (HIV) that causes?AIDS?.
Infupertide belongs to a group of medicines that work by blocking the binding of the virus to its host cell CD4, which prevents virus replication.
Infopertide is taken with other antiviral drugs to prevent the development of resistant strains of the virus. Infopertide is usually given to patients who have not responded to prior antiviral therapy.
Papaverine has been in use since 1937, as it relaxes smooth muscles and relieves pain arising from contractions of soft muscles in part of the small intestine and in the sexual and urinary systems.
This drug was previously used to treat peripheral vascular diseases and transient ischemic attacks (transient ischemic attacks) affecting the brain. However, due to the lack of effectiveness of papaverine for the treatment of these conditions, and due to the development of other drugs, the use of this drug was stopped to treat these conditions.
An intravenous injection of papaverine can be given in cases of acute colic, such as episodes of?renal colic,??and papaverine is used to treat erectile dysfunction in men by papaverine injections.
Among the most important side effects of this drug: Intestinal disturbances, headaches, and in rare cases, jaundice.
Paracetamol, or as it is known by its other name, acetaminophen, has been known since the beginning of the last century, but its use as a pain reliever began in the fifties of the last century.
Paracetamol belongs to the group of pain relievers and non-narcotics. It is among the home medicines that are used to relieve mild and moderate pain and reduce fever. This medicine is suitable for the use of adults and children.
One of the advantages of using paracetamol is that it does not cause stomach problems or bleeding;?Therefore, it is suitable for people who suffer from peptic ulcers or people who are not suitable for the use of aspirin, and this drug can also be used with anticoagulant drugs, but it is necessary to be careful not to take it in large doses.
Paracetamol overdose is dangerous and can cause severe damage to the liver, and large doses can be toxic to people who regularly consume alcoholic beverages, even in small amounts.
Paroxetine is an antidepressant that belongs to a group of medicines called selective serotonin reuptake inhibitors (SSRIs).
It treats depression and other mental illnesses by increasing the amount of serotonin, a natural substance in the brain that helps maintain mental and emotional balance.
Paromomycin?is an aminoglycoside antibiotic and?methylbenzethonium chloride?is a disinfectant.?This combination of the two drugs is used in the topical treatment of skin lesions typical of?Leishmaniasis?, an infection caused by a parasite transmitted by Phlebotomus
Paricalcitol is a synthetic analogue of vitamin D. It acts by binding to and stimulating vitamin D receptors in the kidneys, parathyroid glands, intestines and bones, thereby reducing parathyroid hormone (PTH) levels and improving calcium and phosphate balance.
Paricalcitol is used to help prevent and treat secondary hyperparathyroidism in people with stage 5 chronic kidney failure (CKD) who are undergoing dialysis to maintain adequate levels of parathyroid hormone.
It is also used to prevent and treat secondary hyperparathyroidism in patients with stage III and IV chronic renal failure who are not on dialysis.
It is worth noting that the use of Paricalcitol is contraindicated in case of high levels of calcium or vitamin D in the blood.
Bacitracin is an antibiotic that inhibits the building of the cell wall of bacteria and is primarily used to treat skin problems and pneumonia in infants.
In terms of the effect of the drug on bacteria, it has similar efficacy to?penicillin?, however, some of the penicillin-resistant bacteria are sensitive to bacitracin.
Bacitracin is successful in treating external bacterial infections, and is contraindicated to treat infections in deep tissues in adults.
Bacitracin is generally combined with another antibiotic preparation called Polymyxin in the same ointment.
Baclofen is a muscle relaxant that acts on the central nervous system, including the spine.
Relieves spasms and spasms resulting from some diseases, such as:??multiple sclerosis?, spinal injury,?cerebral palsy?, and stroke.
Although this medicine does not cure these diseases, it increases the ability to move with the start of physical therapy
Paclitaxel is a cancer medication primarily used to treat ovarian and breast cancer.
Paclitaxel is also used to treat non-small cell?lung??cancer and Kaposi's sarcoma in people with AIDS
Palonosetron is a serotonin (5-HT3 antagonist) antagonist used to prevent acute and delayed nausea and vomiting caused by chemotherapy or after surgery.
Compared to other drugs from the same family, palonosetron is the first drug of its kind that is able to prevent existing nausea and vomiting, that is, that appears within 24 hours of receiving chemotherapy, and it can prevent nausea and vomiting that appear at a later stage of treatment.
In general, the side effects of palonosetron are very minor, the most common being headache and constipation.
Paliperidone is an atypical antipsychotic that changes the activity of certain natural substances in the brain.
This medication is used to treat??schizophrenia??in adults and adolescents who are at least 12 years old, and paliperidone extended-release injection is used alone or with other medications to treat schizoaffective disorder in adults.
Paliperidone, as other drugs belonging to this group, does not cure the patient, but rather relieves the symptoms.
Paliperidone should not be used to treat?mental disorders?caused by dementia.?Because it may increase the risk of death.
Palivizumab is an antibody that has been extracted from men who have been exposed?to?RSV - Respiratory syncytial virus of the lower airways.
Palivizumab is a medicine that is used specifically for children and under two years of age to prevent infection with respiratory syncytial virus. It is worth noting that this medicine is not effective for treating the virus after infection.
This virus causes serious lung problems in premature babies or babies with congenital heart and lung disease.
Warfarin is an anticoagulant, in other words, this drug is used to prevent blood clots from forming, especially in areas where blood flows slowly, such as the veins in the legs and pelvis. Pulmonary hemorrhage, which can cause death.
Warfarin is also used to reduce the chance of??heart?clots forming in people with??atrial fibrillation?or in those who have had an artificial heart valve implanted. These clots may reach the brain and cause a stroke.?
Warfarin is a commonly used drug and requires regular monitoring of its use in order to ensure an appropriate maintenance dose. Since the full positive effects of warfarin do not appear until after 2-3 days, the patient is usually given a rapid-acting anticoagulant such as heparin, in order to The effect of warfarin is supplemented at the beginning of treatment.
As with most anticoagulants, the most serious side effect of warfarin is the risk of excessive bleeding, which is usually caused by an overdose
Hydroquinone is an effective drug for lightening the color of dark skin spots, which works by slowing the production of melanin in the skin, hydroquinone is used to treat hyperpigmentation of the skin such as: chloasma, freckles, and spots that appear as a result of acne (Acne).
Avoid exposure to sunlight when using the drug and use sunblock. It is recommended to continue using sunblock after treatment with hydroquinone to avoid re-pigmentation of the skin.
Hydrocortisone is chemically similar to the hormone cortisol, which is produced by the adrenal glands, and one of its most important uses is to replace natural hormones in the case?of adrenal?insufficiency.
The main use of this drug is to treat a variety of inflammatory and allergic conditions. When used topically, it leads to immediate relief of inflammation of the skin, eyes, and outer ear. It is taken orally for the treatment of asthma, inflammatory diseases in the intestine, cases of?allergic?response, and rheumatism. Injecting it directly into the joint relieves pain and stiffness.
One of its most important uses is to prevent serious asthma attacks, but excessive use of hydrocortisone creams can cause permanent skin atrophy, and when oral hydrocortisone is taken for a long time and in high doses, it can lead to dangerous side effects and suppression of the immune system.
Hydrochlorothiazide is a drug that belongs to a group of thiazide diuretics that remove excess water from the body and reduce fluid accumulation known as edema in people with the following conditions:
?Congestive heart failure?.
Kidney disease.
Cirrhosis?of the liver.
Premenstrual syndrome.
Hydrochlorothiazide is often used to treat high blood pressure, and since this medicine lowers the level of calcium in the urine, it's sometimes used to prevent certain types of kidney stones from recurring.
Hydrochlorothiazide increases the loss of sodium in the urine, which may lead to the emergence of many symptoms, and increases the risk of developing heart rhythm disturbances (arrhythmias), especially when taking drugs such as digoxin, and therefore potassium (Potassium) is often given and added to the patient. with hydrochlorothiazide.
Hydroxyurea belongs to a class of medicines called antimetabolites.
Hydroxyurea is used alone or in combination with chemotherapy or radiation to treat a certain type of??chronic myelogenous leukemia??(CML). It also helps treat ovarian cancer and head and neck squamous cell carcinoma, a type of skin cancer.
The drug's anti-tumor effects are due to its ability to damage the genetic material of cancer cells, thus preventing their development and reproduction, which ultimately leads to the death of these cells.
Hydroxyurea is also used to reduce pain and the need for blood transfusions in people with sickle cell anemia by helping to prevent the formation of sickle-shaped red blood cells, but it does not cure sickle cell anemia.
Hydroxychloroquine is primarily given to prevent and treat?malaria??but is not effective against all types of malaria.
It is also usually given in combination with other drugs to treat a number of autoimmune diseases, such as: systemic lupus erythematosus and rheumatoid arthritis. Hydroxychloroquine treatment for these diseases is usually given as a second line after the failure of the first-line drugs. in treating these diseases.
The drug is effective in patients with SLE against skin symptoms, and against arthritis.
Hydroxychloroquine is not intended for prolonged use in children and is permitted in patients with G6PD deficiency, but should be used with caution in these patients;?Because it and other antimalarials can cause?hemolytic?anemia in these patients.
Hydroxyzine is a sedative drug that does not belong to the family of phenothiazines or benzodiazepines?. It is used to calm and relieve acute anxiety. In addition, it has the following effects:
Antihistamine effect.
Effect on the widening of the airways (Bronchodilator).
Antiemetic effect.?
Because of these properties, it is often used to treat severe allergies or asthma patients who suffer from severe anxiety, and because of the anticholinergic effect, this drug causes side effects including drowsiness, dry mouth and urination disturbances.

This medication is available in a variety of over-the-counter products to relieve stomach acid,?indigestion?, and ?heartburn.
This medicine also acts as a laxative to treat constipation by absorbing water from the blood vessels surrounding the intestine into the intestine, thus stimulating bowel movements and softening the stool to facilitate its passage.
Magnesium hydroxide is not usually used as the sole ingredient in antacid preparations due to its laxative effect, but rather it is combined with aluminum hydroxide, which causes constipation and eliminates the laxative effect of magnesium hydroxide.
Aluminum hydroxide has been used for more than 50 years as a stomach antacid, and is a key ingredient in most over-the-counter (OTC) remedies for acid reflux and indigestion.
Since it is constipating in some cases and may be used to reduce diarrhea, it is usually combined with magnesium-containing antacids to counteract the diarrheal effect of magnesium.
Aluminum hydroxide is characterized by its long activity, so it is very successful, especially in the treatment of gastric and duodenal ulcer pain or inflammation of the esophagus with GERD, and also helps in the treatment of ulcers.
Hydralazine is a drug to lower high?blood?pressure. Hydralazine dilates blood vessels and is usually used to treat moderate to severe cases.
Hydralazine is given by tablets, but in emergency cases it can be given by intravenous injection due to its rapid effect.
Hydralazine is usually given as an add-on to diuretics or beta blockers.
Although chloral hydrate has been in use for more than one hundred and fifty years, its luster has not faded yet;?Because it is used mainly as a sedative and hypnotic in the elderly and children in particular, but until today the mechanism of its effect is not fully known. One estimate says that this drug turns into alcohol that inhibits the wake and sleep centers in the central nervous system.
Chloral hydrate is used to calm?children?and young children before painful examinations. Common side effects of this drug include allergic reactions and, in rare cases, it may cause irritation rather than drowsiness. Chloral hydrate is being replaced in many places by short-acting benzodiazepine preparations.
Methenamine hippurate, also known as hexamine hippurate, is a long-term antibiotic used to treat and prevent recurrent urinary tract infections.
The drug is taken by tablets and absorbed in the digestive system and reaches the urinary tract, where it is broken down into ammonia and formaldehyde, the effective substance responsible for killing germs.
The active ingredient is only released if acidic urine is present, so your doctor may recommend drinking certain types of fluids, such as cranberry juice or other medications to make your urine more acidic.
Hypericum is not chemicals but an extract from the herb called Hypericum perforatum?,?also known as St. John's wort, a plant with a long history of medicinal use.
Therapeutic uses of hypercum
The central use of hippocum plant extract is to treat the following conditions:
depression?.
anxiety.
Sleep disorders.
Reviewed clinical studies?have?compared the efficacy of Hypericum to other antidepressants, such as Citalopram,?Paroxetine?, Imipramine, Amitriptyline, and Fluoxetine.
Synthetic HMG is a human menopausal gonadotrophin extracted from the urine of?postmenopausal women?, and contains two hormones: luteinizing hormone (LH) and follicle-stimulating hormone (FSH).
This hormone stimulates the growth of follicles in the ovary when used to treat fertilization problems in women who suffer from ovarian failure. It also helps fertilize an egg and helps in the early stages of fetal development.
HMG is also used to treat men who have a problem with the pituitary gland and who have a problem with sperm production.
Nevirapine is an antiviral medication used to treat patients infected with the human immunodeficiency virus (HIV) that causes AIDS in adults and children 15 days of age or older.
This drug belongs to the group of non-nucleoside reverse transcriptase inhibitors (NNRTIs), and thus prevents the replication and reproduction of the virus in the body, and is usually taken with other drugs that inhibit the virus.
But it is worth noting that nevirapine does not cure HIV, and it should not be used to prevent it, but it may reduce the chance of developing acquired immunodeficiency syndrome or AIDS and diseases related to HIV, such as: serious infections or cancer.
Neomycin is an aminoglycoside antibiotic.
Common uses of neomycin
Neomycin is used in the following cases:
skin infections;
Eye and ear infections.
Preparation for operations and gastric emptying.
Hepatic?coma.
Hepatic encephalopathy.

Nimesulide belongs to the group of modern non-steroidal anti-inflammatory drugs (NSAIDs).
This medicine is used to relieve pain caused by inflammation, such as: cases of?osteoarthritis?, inflammation in muscles or tendons, and acute pain caused by other causes, such as: menstrual pain.
Nimodipine, which belongs to a group of calcium channel blockers, is used to prevent and treat neurological deficits caused by narrowing of blood vessels in the brain.
Nimodipine dilates the blood vessels, especially those in the brain after a subarachnoid hemorrhage, where the blood vessels in the brain narrow, which can lead to paralysis or other neurological problems.
Common side effects of the drug include headaches, flushing of the face, nausea, and spinning sensations following low blood pressure
?Nilotinib?is??a drug used to treat patients with chronic myelocytic leukemia (CML), and is usually given in the advanced stages of the disease or when other medications have not responded to it.?
Nilotinib is taken orally, and its mechanism of action depends on slowing or stopping the spread of cancerous tumors by inhibiting the action of tyrosine kinase enzymes, which is more effective than many drugs in the same group.
Nilotinib may cause many side effects, such as: anemia, blood contamination, infection, nausea, digestive disorders, headaches,?skin rashes?, and low levels of potassium and magnesium in the blood.
Nellarapine is an anti-metabolic cancer chemotherapy that interferes with the growth and spread of cancer cells in the body.
Nellarapine is used in T-cell acute lymphoblastic leukemia and T-cell acute lymphoblastic lymphoma after the disease has returned or after at least two treatment attempts have failed.

Niclosamide is a medicine used to treat tapeworm infections and intestinal flukes.
Niclosamide should not be started if the patient suffers from constipation , but the normal bowel function must be restored and then treatment should be started after that to obtain its full effectiveness.
This medicine is considered relatively safe, due to the absorption of small amounts of it in the digestive system, although it may cause many common side effects, such as: itching, a feeling of heaviness in the head, in addition to diarrhea.
Nifedipine is one of the most common medicines used to treat?heart conditions?and high blood pressure. It belongs to a family of medicines called calcium channel blockers.
Nifedipine is mainly used to treat??high blood pressure,??especially by long-acting tablets, and to treat??angina pectoris??, especially for the treatment of angina caused by coronary artery spasm and patients with heart failure. Nifedipine is also used as an ointment to treat anal fissures.
Nystatin is an antifungal drug that was developed in the early 50s of the last century. Nystatin is effective for treating superficial infections caused by Candida.
Since the body is not able to absorb nystamine from the digestive system into the blood circulation, it is not used to treat infections and cannot be given by injection, side effects from the drug's use rarely occur.
Nedocromil sodium is an anti-inflammatory drug that inhibits the secretion of common inflammatory substances in?asthma?. Nedocromil is administered by nebulizer in patients with mild to moderate asthma.
Nedocromil does not dilate the bronchi, so it is effective in preventing seizures and not in treating seizures after they have occurred and reached their peak;?Therefore, nedocromil is not given to patients during a seizure.
Nitrofurantoin is a fast-acting antibacterial drug used to treat?urinary tract infections??such as cystitis.?Where the drug is concentrated in a high amount in the urinary tract where the germs are located, which can treat the infection within a short time.
This medicine causes side effects in 10% of patients who take it. The most common and unwanted side effect is stomach irritation. This effect can be mitigated by taking the medicine with food.
Nitrazepam belongs to the benzodiazepines family. Nitrazepam is used for the short-term treatment of?sleep?disorders .
Due to the long pharmacological activity of nitrazepam relative to other benzodiazepines, it may increase the likelihood of feeling drowsy or foggy the next day;?This is why nitrazepam is effective in preventing early awakening from sleep.
Niacin is?vitamin?B3 , a drug used in large doses to lower the levels of bad cholesterol (Low-density lipoprotein - LDL) and triglycerides (triglycerides) in the blood. It also contributes to raising levels of good cholesterol (High density lipoprotein - HDL) in the blood.
Niacin is not used alone to lower cholesterol, but is usually given in combination with statins, diet, and physical activity.
Nonoxynol 9 is a spermicide that is used shortly before sexual intercourse to prevent pregnancy, but this preparation is not 100% effective in?preventing pregnancy?, so it is recommended to use it with other methods of contraception, such as: condoms.
This product does not prevent infection with the human immunodeficiency virus (HIV) that causes?AIDS?, or prevent infection with sexual diseases. In addition, the medicine may cause irritation in the vagina, which increases the possibility of infection with HIV or other sexual diseases from the infected husband.
Norethisterone is given alone or with estrogen to treat gynecological conditions such as irregular menstruation, heavy menstrual bleeding, and endometriosis.
One of the common uses of this drug is to delay the occurrence of menstruation, and there is another use in large doses for the treatment of breast cancer, but before starting treatment with Norethisterone, the patient must undergo a thorough gynecological examination to ensure that there is no pregnancy.
Norfloxacin, a quinolone antibiotic, has been in use since 1986, when it is used to treat infections in the urinary tract.
There is a similarity between the composition of norfloxacin and nalidixic acid used 40 years ago to treat infections in the urinary tract, but the difference between them is that the effectiveness of norfloxacin has a wider range of bacteria, and there are those who use norfloxacin to treat?gonorrhea??and bacterial enteritis, but these days this antibiotic is used in Only for veterinary purposes.
The main side effects of norfloxacin are nausea, headache, and in rare cases, especially at high doses, crystals can form in the kidneys.
Nortriptyline?is a member of the tricyclic antidepressants family, used to treat?depression .
It works by increasing the amounts of certain neurotransmitters in the brain that may be out of balance in people with depression
Nefazodone is a medication used to treat?depression?and may be of benefit to patients who have experienced side effects from other antidepressants.
The principle of action of the drug depends on preventing the absorption of certain neurotransmitters from the blood, namely: serotonin and norepinephrine.
Nalidixic acid is an antibacterial medication used to treat urinary tract infections.?Sometimes it is used to prevent recurring urinary tract infections.
When this drug is taken orally, it does not accumulate in the body's tissues, but rather concentrates in the urine nalidixic acid, which is effective against strains of bacteria common in urinary tract infections.?Some bacteria can quickly develop resistance to it, so using it a second time when the infection is still going is less effective.
Naloxone is an opioid antagonist such as morphine, pethidine, oxycodone, and codeine, and is used primarily in cases of opioid overdose that depress the central nervous system and respiratory system.
It is important to know that naloxone is used primarily in cases??of opioid poisoning?, while naltrexone, another opioid receptor antagonist, is used to help treat opiate addiction.
Naltrexone is a substance that has opioid antagonism and can treat opium addicts or opium poisoning.
Naltrexone blocks the receptors to which opiates bind and block their activity, thus preventing the euphoria that characterizes the use of these substances.
Another common treatment for naltrexone is by detoxification. According to this method, naltrexone is injected in high doses while the patient is under anesthesia to prevent symptoms, and then the patient receives oral naltrexone for daily use.
Naratriptan is a?migraine?medication ?with a chemical structure similar to serotonin, which selectively acts on a specific group of serotonin receptors, and leads to the constriction of blood vessels in the brain, and researchers believe that this activity is responsible for alleviating headaches.
Natalizumab is used to treat multiple sclerosis, as it blocks the passage of white blood cells into the central nervous system that destroy myelin cells, and natalizumab slows the natural progression of physical disability caused by the disease while at the same time decreasing The frequency and severity of episodes of this disease.
Natalizumab is also used to treat moderate to severe Crohn's disease.
Nabumetone is a non-steroidal anti-inflammatory drug (NSAID) that stops the body's production of prostaglandins that cause pain, fever and inflammation at the site of the injury.
Nabumetone is used to relieve pain, swelling, and stiffness caused by?osteoarthritis?,?rheumatoid arthritis?, and similar conditions that require anti-inflammatory treatment.
Mupirocin is an antibiotic used as a topical treatment for bacterial skin infections, by inhibiting the synthesis of proteins important for the growth and reproduction of bacteria, leading to their elimination.
Mupirocin ointment is used topically on the skin to treat Impetigo, and it is also used to treat secondary bacterial infections of?Staphylococcus Aureus and?Streptococcus pyogenes?in?wounds and skin lesion
Minoxidil is a vasodilator that relaxes the muscles in the walls of arteries and blood vessels, causing them to widen and improving blood flow.
Minoxidil is used to treat severe high blood pressure that is causing symptoms or damage to vital organs, and it is usually given with other medications to reduce serious side effects.
Minocycline is a tetracycline antibiotic that treats infections by preventing the growth and spread of bacteria.
Common Minocycline Uses
Minocycline is primarily used to treat??acne??(acne) by eliminating the bacteria that inhabit the pores and reducing the skin's natural oils that cause inflammation and pimples.
Minocycline is also used to treat many different bacterial infections, such as:
severe acne;
Urinary tract infections.
Respiratory infections.
skin infections;
chlamydia;
tick fever;
gonorrhea;
syphilis;
eye infections;
Lymphatic system infections.
Infections of the intestine and reproductive system.
Other bacterial infections in people allergic to penicillin.
Meningitis.
Memantine is a drug for the treatment of dementia caused by??Alzheimer's?given to treat patients in the middle or advanced stage of Alzheimer's disease, and it has also been found to be effective in the treatment of advanced vascular dementia.
Milnacipran is an antidepressant drug belonging to the family of selective serotonin reuptake inhibitors that in addition to increasing the amount of serotonin it also increases the amount of noradrenaline in the brain.
Miconazole is an antifungal medication that has been popular since the 1970s and works by stopping the growth of the fungus causing the infection.
Common uses of miconazole
Miconazole is used to treat the following conditions:
Candida infection inside the mouth and throat.
Vulvovaginal candidiasis.
Tinea infection of the skin, such as: ringworm, tinea cruris, tinea pedis, and tinea versicolor.
Mycophenolate Mofetil is a drug that suppresses the immune system, and it converts in the body to the active compound Mycophenolic Acid, which prevents the reaction of the body's immune system against the transplanted organ.
Mycophenolate mofetil is given in combination with cyclosporine and corticosteroids to help prevent the immune system from attacking the transplanted organ in people who have had heart, liver or kidney transplants.

Misoprostol is a prostaglandin-like drug that reduces stomach acid secretion and protects the stomach lining.
Misoprostol is primarily used to prevent irritation and?peptic ulcers??in the stomach caused by taking non-steroidal anti-inflammatory drugs (NSAIDs), such as: aspirin, ibuprofen, and naproxen, which are used to treat arthritis or relieve pain in general.
The most common side effect is diarrhoea. Misoprostol may cause uterine contraction, miscarriage or premature labour. Therefore, this medicine should not be taken during?pregnancy?and it is advisable to stop using it before becoming pregnant.
Thanks to this feature, Misoprostol is used for abortions within 70 days of pregnancy, alone or in combination with Mifeprestone.

Mesalamine is an anti-inflammatory drug for the gastrointestinal tract. The most common clinical use is to treat inflammatory bowel diseases, especially??ulcerative??colitis and Crohn's disease.
The difference between the drug forms used to treat these diseases is slight and often without clinical significance, but if the disease affects the anus only, the drug can be taken by suppository or enema.

Mizolastine is?a long-acting antihistamine, and it is mainly used to treat nasal infections, especially??hay fever?, and it may also be useful in treating other types of allergies such as urticaria. for example.
Mizolastine helps relieve allergy symptoms, such as: sneezing, and irritation in the eyes and nose, and is not accompanied by depressant effects on the central nervous system.
Some?clinical research?indicates that mizolastine is more effective when compared to loratadine in the treatment of allergy symptoms, but it is associated with serious side effects such as heart rhythm disturbances (Arrhythmias). Unlike loratadine, it does not cause such effects.?Therefore, mizolastine is contraindicated in patients with arrhythmias or any other?heart disease?.

Mercaptopurine (MP) is a drug used to treat leukemia, especially acute lymphocytic leukemia and acute myeloid leukemia. This drug belongs to a class of substances called anti-metabolites, as these substances block the building blocks of cancerous cells, preventing their development.
Mercaptopurine is also used to treat autoimmune diseases such as Crohn's disease, ulcerative colitis, and lupus.
Like other anti-cancer drugs, mercaptopurine suppresses the production of various blood cells in the bone marrow, which causes anemia. Patients are also more susceptible to infections and abnormal bleeding.

Mirtazapine is a 4-cyclic antidepressant that blocks alpha-2-adrenergic receptors in the brain, increasing the release of norepinephrine and serotonin in the brain.
In addition, this drug works by inhibiting subtypes of serotonin receptors, which in turn contributes to restoring chemical balance in the brain.
Mirtazapine is primarily used to treat major depressive disorder (MDD) in adults.

Midodrine is?one of the drugs used to treat? orthostatic?hypotension??, which occurs when moving from one position to another, and it may also sometimes be used to treat stress incontinence, where its mechanism of action depends on the narrowing of peripheral blood vessels. Which leads to an increase in blood pressure.
Midodrine may cause a significant increase in blood pressure, especially while lying down. Therefore, it is recommended to take the dose at least 4 hours before bedtime, and blood pressure should be monitored during the treatment period.

Medroxyprogesterone is a progestin that is a form of progesterone, a synthetic female sex hormone similar to the natural hormone that helps regulate ovulation and menstruation.

Megestrol is a hormonal anti-cancer drug that is used to treat advanced?breast?cancer and endometrial cancer. Megestrol is also used in rare cases to treat?prostate?cancer.
Megestrol is similar to the female hormone progesterone, so it prevents ovulation and uterine contractions, and is an anti-androgen, but its exact mechanism of action against cancer is not yet fully understood.
Since megestrol has an appetizing effect, it may help people who suffer from loss of appetite or who suffer from weight loss due to advanced cancer, and indeed it is used as a suspension in large doses to treat anorexia or weight loss due to cancer or AIDS ( AIDS).

Methmazole is?one of the drugs that is used to treat some problems, such as: hyperthyroidism and?Graves?' disease, and it is also used before surgery to remove part of the thyroid gland in order to prevent side effects caused by high levels of thyroid hormones.
Methimozil's mechanism of action is to reduce the production of thyroid hormones by blocking the fusion of an iodine molecule with a protein called thyroglobulin.
The treatment may cause some side effects, such as: Leukopenia,?sore throat?, fever, and cough, in addition to oral pain.

Methylprednisolone is a synthetic corticosteroid.

Methylergometrine is a drug belonging to the alkaloid family, and is mainly used to prevent uterine bleeding after childbirth or abortion. The mechanism of action of methylergometrine is to increase the contraction of the smooth muscles of the uterus, which reduces the severity of uterine bleeding.
Taking methylargoth may cause many side effects, such as: nausea, vomiting, abdominal pain, headache, high blood pressure,?angina pectoris?, pain in the hands and legs, cramps, and coma.

Methotrexate is an anti-metabolite that interferes with the growth of some cells of the body, especially cells that multiply rapidly, such as: cancer cells, bone marrow cells, and skin cells.

Methazolamide is an intraocular hypotensive drug intended for the treatment of?glaucoma?.
Methazolamide belongs to a group of drugs that inhibit carbonic anhydrase enzymes, such as acetazolamide. The function of this enzyme is to produce bicarbonate and hydrogen ions from carbon dioxide and water.
Bicarbonate is necessary in order to produce the aqueous fluid in the eye behind the cornea, blocking the enzyme and then decreasing the concentration of bicarbonate leads to relief from the increased intraocular pressure that is characteristic of glaucoma.
In the kidneys, methazolamide increases the excretion of bicarbonate with other salts, which leads to the polarization of more water from the body, which is excreted in the urine. However, the diuretic activity of this drug is relatively low.
Methazolamide, like acetazolamide, can be used to prevent symptoms of?Altitude Sickness?.

Methadone is an opiate medication that is used to relieve moderate to severe aches, such as post-operative aches and chronic diseases?such as cancer?.
Methadone is used as a treatment for drug addicts, as the effect of its continuous use, which ranges between 22-48 hours, prevents the emergence of addiction symptoms, and reduces the desire to use.
The mechanism of the effectiveness of methadone to relieve pain is that it binds to opiate receptors in the brain and in smooth muscles to relieve pain.
Methadone may cause serious disorders up to the point of life threatening, including: disturbances in the rate of heartbeat??and?disturbances in breathing, which requires tracking and monitoring of the activity of the heart, lungs and liver during the use of methadone.
Also, taking methadone for long periods of time may develop a tendency to become attached to and become addicted to it.

Metolazone is a diuretic medication that helps prevent the body from absorbing too much salt, thus reducing the amount of water and salt in the body by increasing the amount of urine, which reduces fluid retention.
Metolazone is used to treat fluid retention or edema caused by a buildup of water and salts in people with??congestive heart failure??or kidney disease.
Metolazone is also used to treat high blood pressure either alone or with other medications.

Metoclopramide has a direct effect on the digestive system, as it works by accelerating the movement of food through the stomach and intestines by increasing the contractions of the muscles of the upper digestive tract.

Metoprolol, used since 1978, is a beta-blocker and belongs to a class of medications called beta-blockers. It works by dilating blood vessels and slowing the heart rate to improve blood flow and lower blood pressure.
In contrast to other beta-blockers that act on the heart and lungs, metoprolol is cardio-selective, meaning it acts primarily on the heart.
From here stems its great value in people who suffer from asthma (Asthma),?bronchitis?(Bronchitis) or other lung diseases, but there is a need to use means of caution in these cases.
Metoprolol also affects the body's response to low blood sugar, which can be a problem in people with diabetes.?

Metformin is a drug belonging to the biguanide group for the treatment of type 2 diabetes, which occurs as a result of the body's inability to use insulin normally, and therefore cannot control the level of blood sugar.
Metformin lowers the level of sugar in the blood by reducing the absorption of glucose from food, decreasing its production by the liver, and enhancing the sensitivity of the body's cells to insulin, which is responsible for controlling blood sugar levels.
The use of metformin is accompanied by a diabetic diet and exercise, and in most cases metformin is used with insulin or other medications to treat diabetes.

Mebendazole is an anthelmintic drug that kills newly hatched worms larvae by preventing them from growing or multiplying in the body.
It is used to treat several types of worm infections, such as:
Whipworm.
Pinworms.
Roundworms.
Hookworms.
Due to the wide range of effectiveness of the drug, it is used for mixed infections caused by several worms, or if the type of worm is not recognized.
With a highly contagious pinworm infection, it's important to treat the whole family together.?

Mephydrolin is an antihistamine used to treat?allergic reactions?such as allergic rhinitis, allergic dermatitis, hay fever, urticaria, conjunctivitis, allergic asthma, eczema, itching, and insect bites.

Mebeverine is a muscle relaxant and antispasmodic drug that acts directly on the smooth muscles of the digestive tract to relieve painful cramps.
It is used to treat symptoms associated??with??Irritable Bowel Syndrome, such as: pain, cramps, abdominal cramps, diarrhea, constipation, and flatulence.
It can also treat some other conditions that have similar symptoms, such as: chronic irritable bowel, spastic constipation, mucous colitis, and spastic colitis.
It is recommended that treatment with medication be accompanied by dietary changes, such as: a high-fiber diet, and sometimes psychotherapy.

Mianserin, a serotonin and antihistamine drug, is an older drug intended for the treatment of depression but is also suitable for the treatment of anxiety disorders or depression associated with anxiety disorders.?Because it tends to cause drowsiness, it is particularly suitable for those who suffer from insomnia, as it has sometimes been found to improve sexual performance that can be compromised by fluoxetine treatment.
The main side effects of mianserin are dry mouth, blurred vision, constipation and dizziness, which in very rare cases can cause a decrease in the number of white blood cells so it is necessary to have regular checkups.

Montelukast is a leukotriene receptor antagonist (LTRAs) that inhibits the activity of chemicals called leukotrienes, which play an important role in allergic and inflammatory responses.
Inhibition of this activity prevents constriction of the bronchi and improves the main symptoms of asthma which include coughing, difficulty and shortness of breath, and chest pressure.

Mometasone is a drug belonging to the corticosteroid group, and it is used to treat diseases caused by infections or allergies. The drug is used to treat various types of skin infections, such as: atopic dermatitis, contact dermatitis, and alopecia. Alopecia areata), eczema, itching, and others.
Mometasone is also used as a nasal spray to treat seasonal allergic rhinitis, or to treat allergies caused by pet dander or house dust mites.?
Excessive use of mometasone, like other corticosteroid medicines, leads to permanent sagging of the skin.?

Moxifloxacin is a quinolone antibiotic used to treat various types of infections caused by bacteria sensitive to this type of antibiotic.
Moxifloxacin eye drops are used to treat infections that affect the eye, and moxifloxacin tablets or intravenous solution are used to treat infections that cause?pneumonia?(pneumonia), and they are used to treat skin infections.
The high efficacy of moxifloxacin makes it possible to take equal doses orally and intravenously.

Morphine is a drug used since the nineteenth century that belongs to a group of medicines called opiate pain relievers or Narcotics, which are derivatives of opium extracted from the immature seeds of the poppy plant.
Morphine works by changing the way the brain and nervous system respond to pain.
Morphine relieves moderate to severe pain that may be caused by injuries, surgeries, heart attacks or chronic diseases, such as: cancer. Morphine can also be used as a preoperative treatment to reduce alertness and anxiety.
Morphine leads to a state of habituation and, in some cases, increased attachment and addiction. However, most patients who take morphine for short-term pain relief do not develop dependence and are able to stop taking the drug without difficulties.

Modafinil is?a drug that activates the central nervous system, and is used to treat symptoms of excessive sleepiness caused by some disorders, such as:??Narcolepsy??, Obstructive Sleep Apnea, and ADHD - Attention Deficit Hyperactivity Disorder ), in addition to??sleep problems??resulting from working for long periods (SWSD - Shift Work Sleep Disorder).?
Modafinil does not cause the euphoria and dependency of other stimulant drugs because its mechanism of action is limited to specific areas of the brain. Headache and nausea are among the most common side effects of this treatment.

?Tissue plasminogen activator (TPA) or the anticoagulant drug Alteplase is an enzyme that breaks down blood clots that can block arteries and is extracted using a genetic engineering technique.
It is generally given intravenously for several hours after the clot has dissolved and dispersed to prevent additional clot formation, after which anticoagulant therapy is given.

Mefloquine is an?antimalarial drug?used to prevent and treat the parasite that causes malaria.
In the event that mefloquine is used to treat active malaria parasites (Plasmodium vivax) in the acute stage, then another treatment must be added, such as: Primaquine to eliminate the parasite from the liver.
Many people who travel to the tropics take this medication for prevention before travel, and in most cases it is well tolerated.

Mesterolone is a synthetic male androgen similar to dihydrotestosterone (DHT - Dihydrotestosterone), which is used in elderly men with low testosterone.
Another use of mesterolone is in the treatment of fertility problems in men with hypogonadism, but it??is not effective for stimulating muscle development.
During the course of treatment with Mesterolone, regular examinations of the prostate should be performed, and the level of liver enzymes should be checked.

Methylphenidate is a central nervous system stimulant.

Methyldopa is one of the most common medications for lowering high blood pressure, and a diuretic is often added to it to enhance its effect and reduce fluid retention.
Other medications to lower high blood pressure, such as??hydralazine?and a beta blocker, are sometimes added to get more effective lowering of high blood pressure.

Metronidazole is an antibiotic in a class of medications called nitroimidazole antimicrobials. It works by killing the bacteria and parasites that cause infection.

Malathion is an insecticide and antiparasitic used to treat infestations caused by head?lice??. It belongs to a class of medications called liceicides, and it works by killing lice.

Maraviroc is an antiviral medication used to treat people who are infected with the human immunodeficiency virus (HIV) that causes?AIDS?.
Maraviroc belongs to the family of drugs that work by blocking the receptor that is located on the outer surface of the cells targeted by the virus.
Because the drug is relatively new, there is a good chance that it will be effective for treating resistant viruses, but in all cases Marviroc is taken with other antiviral drugs to avoid the development of resistant strains of HIV.
As for the safety of using the drug, the drug is well tolerated by the majority of patients.

Maprotiline belongs to a class of medicines called tetracyclic antidepressants.
It works by increasing the amounts of certain brain chemicals that may be out of balance in people with depressive disorders, helping to improve mood, restore appetite and renew interest in daily activities.
Maprotiline is used to treat depression, depressive neurosis, and anxiety associated with depression. This medicine is also effective in treating depression that appears as part of bipolar disorder or manic depression.
Similar to tricyclic antidepressants, maprotiline may cause arrhythmias and is therefore used with caution in people with heart disease. This medicine is usually not given to patients with epilepsy, because the medicine may lead to seizures.

Linezolid is effective against pneumonia, skin and tissue infections, and infections caused by Enterococcus bacteria.
Treatment with linezolid is only in cases where bacteria are suspected of resistance to other antibiotics and it is important to understand that indiscriminate use of these antibiotics leads to rapid development of resistant bacteria as well.
Linezolid is a weak, non-selective MAOI-oxidase inhibitor and should not be used with foods or beverages containing thyramine or with adrenergic preparations.

Linograstim is a drug produced by genetic engineering that works in a similar way to a protein in the body called granulocyte colony stimulating factor. This protein helps the bone marrow to produce?white blood?cells, ?especially neutophil cells, at a high rate.
This drug is also suitable for treating persistent and difficult?neutropenia??that can be congenital, or of unknown origin, and cause recurrent episodes of infection.
There are cases in which lenograstim is used before chemotherapy in high doses to help the bone marrow increase the production of osteoprogenitor cells, in order to collect excess bone cells and return them to the body after chemotherapy to produce new blood cells.
Lenograstim is also used after a bone marrow transplant.

Lindane, also known by its chemical name, Gamma Benzene Hexachloride, is an insecticide, and is an antiparasitic drug that lives or lays eggs in the skin or hair.
It is used to treat?scabies??, head lice and pubic lice. Lindane kills parasites, so it is used for treatment only in case of infection, and is not used for prevention cases.
Lindane should be used only in patients who cannot take other medicines or other options have failed to work.
Avoid contact with eyes and open wounds. It is toxic if swallowed.?

Lenalidomide is a drug that belongs to the immunomodulatory agents and is an analogue of thalidomide. It works by helping the bone marrow produce normal blood cells and kill the abnormal cells in it.
It also reduces the process of new blood vessel formation (angiogenesis) that nourishes cancer cells

Levetiracetam is a class of anticonvulsant medication that works by decreasing abnormal activity in the brain. It is used with other medications to treat certain types of seizures in adults and children with epilepsy.
It is used in the treatment of partial seizures in adults and children of different ages, depending on the type of preparation used.
It is also used with other seizure medicines to treat tonic-clonic seizures in people who are at least 6 years old, and myoclonic seizures in people who are at least 12 years old.

Levonorgestrel is a synthetic hormone that acts similar to progesterone in the body. Levonorgestrel is used as an emergency??contraceptive??by preventing ovulation, in addition to making the vaginal fluid thicker, which prevents sperm from reaching the egg.
The treatment is used in a high dose if the marital relationship took place without any method of contraception, within 72 hours after sexual intercourse, and it is also used in cases of forgetting to take at least two doses of the contraceptive pill.
It is important to know that the treatment can be used as an??emergency?contraceptive ?for those over 16 without a prescription.
The effectiveness of the treatment increases the sooner it is taken after intercourse, while it decreases in some other cases, such as: vomiting up to 3 hours after taking it, or taking other medications that speed up its analysis in the liver.
Levonorgestrel is also present in low doses in the contraceptive pill and intrauterine device, where small amounts are secreted daily into the uterine cavity.
Taking levonorgestrel may cause many side effects, such as: nausea, and menstrual disorders.

Levopromazine is an antipsychotic drug belonging to the family of phenothiazines used to treat schizophrenia, bipolar disorder and depression.
Compared with other antipsychotics of the phenothiazines family, levomepromazine has relatively low antipsychotic efficacy, but antinausea and emetic efficacy and analgesic potential;?For this reason, levomepromazine is used in low doses to relieve moderate to severe pain and to treat nausea and vomiting caused by certain medications, radiotherapy, and anesthesia.
Levopromazine also has an anticholinergic effect, but causes drowsiness, blurred vision and dry mouth, so caution should be exercised when administering it to people with glaucoma.
Levopromazine may also cause orthostatic hypotension, which is a drop in blood pressure when moving from a lying or sitting position to a standing position.?Therefore, at the beginning of the treatment, the patient must lie down for about an hour after taking the medicine.

Levocapstin is an antihistamine that treats??allergies?by selectively blocking type 1 histamine receptors.
This medicine is used as a nasal spray to treat symptoms associated with allergic inflammation in the nose, such as: runny nose, sneezing, and irritation caused by allergies, and it is used as eye drops to reduce irritation caused by allergic conjunctivitis.

Levofloxacin is a fluoroquinolones antibiotic used to treat various types of infections caused by sensitive microorganisms.
It is used to treat the following bacterial infections:
bronchitis.
Sinus infections.
Urinary tract infections.
Pneumonia.
Prostatitis.
skin infections;
Bacterial conjunctivitis.
It may also be used to treat people exposed to anthrax germs or treat and prevent plague, and should only be used for infections that cannot be treated with a safer antibiotic.
The main side effects of this drug are nausea,?abdominal pain?, diarrhea or constipation, and headache.

Levodopa is a medication commonly used to treat Parkinson's disease.
In the body, levodopa is converted into?dopamine?. Loss or insufficient dopamine causes Parkinson's disease, making levodopa a very effective drug.
Levodopa is given alone or added with other medications, such as: Carbidopa, or with Benserazide, which are drugs that increase the effect of levodopa in the brain, and help to give it in lower doses, which also reduces side effects.

Levothyroxine is a synthetic substitute for the natural hormone produced by the thyroid gland, primarily used to correct a deficiency of the hormone when it is not being produced in sufficient quantity.

Lisuride is a drug that directly stimulates dopamine receptors in the brain. It is a dopamine agonist, reduces the production of the hormone prolactin, and stimulates some serotonin receptors.

Lisinopril is a medicine that belongs to a class of medicines called angiotensin-converting enzyme (ACE) inhibitors.
It works by reducing certain chemicals that cause blood vessels to constrict, which helps blood flow more smoothly and the heart can pump blood more efficiently.
It is used to treat patients with?high blood pressure?, patients with congestive heart failure in adults, or to support survival after a heart attack.
Various studies suggest that ACE inhibitors may delay the development of renal failure in patients with?diabetes?that involves excretion of protein in the urine, so the doctor may prescribe medication for this.

Lercanidipine is a vasodilator drug that belongs to the family of calcium channel blockers (CCB) and is used to treat high blood pressure.

Letrozole works by blocking the aromatase enzyme, which contributes to the last stage of estrogen production. There are certain types of estrogen related breast cancers, so blocking estrogen production by inhibiting aromatase by this drug would prevent tumor formation, The?drug is intended to treat?breast cancer?in?postmenopausal women?only.

Pancrelipase is a compound of the following enzymes: lipase, amylase, and protease responsible for the breakdown of fats, starches, and proteins.

Lomefloxacin is a fluoroquinolones antibiotic used to prevent and treat a wide range of bacterial infections caused by susceptible organisms, such as:
bronchitis.
Cystitis.
Urinary tract infections.
skin infections;
Prostatitis.
Salmonella enteric fever.
Gastroenteritis caused by salmonella bacteria.
Shigellosis.
Transurethral resection of the prostate.
Bacterial infections that affect the conjunctiva and eyelids when used as??an eye?drop .

Lovastatin is a drug that helps treat people with high blood?cholesterol?.
Lovastatin lowers the level of bad cholesterol (LDL) and triglycerides in the blood on the one hand, and raises the level of good cholesterol (HDL) in the blood on the other.

Losartan belongs to a group of medicines called angiotensin II receptor blocker. Angiotensin II is a substance in the body that encourages constriction of blood vessels.
So, when blocking its action, the blood vessels expand, which lowers blood pressure and improves blood flow. Therefore, losartan is used in the following cases:
Treating high blood pressure.
Reducing the risk of stroke in some people with heart disease.
Treatment of diabetic nephropathy in people with type 2 diabetes and high blood pressure.
Unlike older generation angiotensin-converting enzyme (ACE) inhibitors, losartan causes fewer side effects, such as coughing,?skin rashes?and changes in the sense of taste.

Lornoxicam belongs to the family of non-steroidal anti-inflammatory drugs (NSAIDs) that have analgesic, anti-inflammatory and antipyretic properties.
Its anti-inflammatory and anti-pain activity results from blocking the action of prostaglandins, which are chemicals that are secreted at the site of injury and cause a feeling of pain and inflammation, and that is through the action of cyclooxygenase (COX) enzymes that produce prostaglandins.
It is used to relieve symptoms of osteoarthritis and rheumatoid arthritis, and lornoxicam is also used for the short-term treatment of mild to moderate pain, such as: back pain, and post-operative pain.
It is worth noting that this drug should not be given to patients with peptic ulcers, severe renal insufficiency and hypersensitivity.

Lorazepam is a medicine that belongs to a group of medicines called benzodiazepines.
It is used to treat?anxiety?and insomnia, anxiety related to depression, to relax muscles and stimulate sleep, and as anesthetic before operations.

Loratadine is a long-acting antihistamine.

Lodoxamide is an anti-allergic drug that belongs to the class of mast cell stabilizers. Its mechanism of action is to block the biological processes in the body that cause allergy symptoms in response to allergens.
Lodoxamide is used in the form of eye drops to treat symptoms of allergy in the eyes, such as: inflammation, itching, redness, burning, and swelling of the eyes.
It should be noted that this preparation contains a preservative that can be absorbed by contact lenses. Therefore, you must remove the lenses before using the preparation and wait at least 15 minutes after using this medication, and then put the contact lenses back in.

Lopinavir with ritonavir is an anti-HIV medication that belongs to the family of protease inhibitors.
The mechanism of action of this drug is to prevent the production of new viruses from the cells that have been infected with the virus. The two compounds that make up this drug have the function of inhibiting the action of the protease enzyme.
In addition, retinavir inhibits the breakdown of lopinavir in the liver and thus increases its time of action and its effect.
As with other anti-HIV medicines, in order to prevent the development of resistant viruses to treatment and to enhance the effectiveness of treatment, this medicine is given in combination with other HIV-suppressing medicines.
It is worth noting that lopinavir with ritonavir will not cure HIV, but it may reduce the chance of developing acquired immunodeficiency syndrome or AIDS and diseases caused by this virus, such as: infection or cancer.

Loperamide is a medication used to reduce???acute and chronic?diarrheal cases.
The drug reduces the loss of water and salts from the intestine and slows down its activity, as a result of which the stools become firmer and the number of stools becomes less frequent.
This medicine is not recommended for diarrheal diseases caused by microbial infection, as it may delay the elimination of harmful substances in the intestine.

The human papillomavirus?(HPV) vaccine is produced?according to a genetic engineering method, by mixing proteins from the virus?s membrane in a way that stimulates the immune system to produce antivirals, without causing disease.?There are two types of vaccine:
a.?Gardasil protects against types 16 and 18, which cause cervical cancer and precancerous growths in the vulva and vagina, and types 6 and 11, which are responsible for precancerous growths and genital warts.?This vaccine has been approved for use in women between the ages of 9 and 26, but it has been shown to be more effective if used before sexual activity begins.
Also, Gardasil has been approved for use in young males aged 9-15 years to prevent infections caused by HPV types 16, 11, 6 and 18.
B.?Cervarix, which is intended for use in women between 10 and 45 years of age, in order to prevent cervical cancer.?It also protects against types 16 and 18, but also provides some protection against HPV types 45, 13 and 52, which together are responsible for some cases of cervical cancer.

The varicella virus vaccine is a live attenuated vaccine?that protects against the varicella-zoster virus.
This virus causes another disease called herpes (?Herpes zoster?), which mainly affects adults.
This vaccination is given to children one year of age and older, and it is recommended to give a second booster dose at the age of six years.
Children who have reached the age of 13 years and over should take two doses of the vaccination, 4-8 weeks apart.
It was found that this vaccination is effective in preventing complications that may result from infection with smallpox, and prevents infection with the disease in about two-thirds of cases, and the remaining third, its members become infected and diseased, but very slightly.
It is forbidden to give this vaccination to those who suffer from a defect in the immune system, since they can become infected with the disease more severely. ??

The pneumococcal?polysaccharide vaccine is a vaccine that can protect against infections caused by a bacterium called Streptococcus pneumoniae.?This germ can lead to invasive diseases such as?otitis media?, pneumonia, meningitis and septicemia.
Vaccination consists of a mixture of polysaccharides for the seven most prevalent types of germs, and it works to stimulate the immune system to produce antibodies to these types of germs specifically, without causing disease.
This vaccine is intended for infants and children from 8 weeks old to 5 years old.
Unlike the Pneumovax vaccine, this vaccine is able to provide protection from opetococcosis in children under the age of two years.
This drug is included in the drug basket for people included in the increased risk groups for pneumococcal infection due to several conditions: malfunctioning of the spleen (eg splenectomy, congenital absence of the spleen and sickle cell anemia), immune disorders (due to malignancy, immunosuppressive therapies and infection with HIV) Acquired Immunodeficiency Virus (HIV).?Organ transplantation,?cerebrospinal fluid leak?with risk of recurring meningitis,?chronic kidney failure?, nephrotic syndrome, or dialysis treatment.

The rotavirus?vaccine is a live vaccine against five types of rotavirus that is given orally.
Rotavirus, a virus that attacks almost all children up to the age of five, is the most common cause of diarrhea among infants and young children.?Its infection rates reach a peak at a generation between four months and two years, and it is especially prevalent in kindergartens and day nurseries, especially during the winter season.
The vaccine is given orally in three stages to children from 6 to 32 weeks of age, so that the first dose is supposed to be given in the period between the sixth to the twelfth week of the child's life.
Mostly, the vaccination is given during the regular periodic visits that children (with their parents) make to the doctor's office, at the age of two months, four months and six months.

Lansoprazole is a drug in the group of proton pump inhibitors in the stomach, which blocks the increase in acid in the stomach.
The drug is given in cases of increased stomach acid, such as: esophageal reflux disease, Zollinger-Ellison syndrome, and stomach ulcers, and as part of the treatment of stomach germs (?H. pylori?).


Lanthanum is??one of the drugs that are used to treat hyperphosphatemia, especially in patients with chronic kidney failure. Its mechanism of action is by binding with phosphate in the intestine, in order to reduce its absorption into the blood and thus reduce its concentrations.
Lanthanum is an effective drug that can be tolerated by patients, unlike other types of phosphate binders, such as:?Aluminum?Hydroxide, which has been found to have toxic effects on the brain and bones.
The side effects of lanthanum include digestive disturbances, such as: constipation,?diarrhea?, head pain, nausea, vomiting, and stomach pain.

Lamivudine is an antiviral drug that is particularly effective against the virus that causes AIDS and??the hepatitis??B virus that causes hepatitis.
The combination of this drug with other drugs that block the AIDS virus, such as zidovudine, leads to a decrease in the amount of viruses in the blood and improves the life expectancy and quality of life of patients, and the drug has an effective role in eliminating hepatitis B virus.

Lamotrigine is used?to treat many disorders such as the following:
Epilepsy,??which can be used with other medications to treat partial seizures, or alone when other treatments fail.
Lennox Gastaut syndrome,??a form of severe epilepsy that appears at an early age and is usually associated with developmental problems.
?Bipolar Disorder??: Lamotrigine is used to stabilize and modify mood in patients with bipolar disorder.
Lamotrigine is suitable for use in adults and children, but it is not usually recommended for use as the only treatment for children under 16 years of age.
In some rare cases,? a severe?skin rash?was observed following the use of lamotrigine for treatment, so the patient in this case must stop taking lamotrigine immediately and go to the hospital to receive the necessary medical treatment. It is also preferable to start taking the drug doses gradually to detect the presence of the condition before it develops.

Lactitol is a substance that stimulates diarrhea. It softens the stool by increasing the proportion of fluid in the large intestine. It is intended to treat constipation that lasts for several days, but it is prohibited to use it in cases of decreased intestinal performance for a day or two, or for other purposes such as purifying the body and others.
Since the drug acts locally on the intestines and is not absorbed into the bloodstream, it is relatively safe to use compared to other drugs that do the same job.

Lactulose is a laxative that softens stool by increasing the amount of fluid in the large intestine.
Lactulose is useful for treating?constipation?, and does not cause laziness in the intestines like other laxatives. In addition, lactulose is used to prevent brain disorders stemming from acute liver failure, due to the ability of lactulose to reduce the level of ammonia in the blood.

Latanoprost is a medication intended for the treatment of glaucoma, which causes increased intraocular pressure. It increases the outflow and drainage of the aqueous fluid in the eyeball and reduces pressure inside the eye.
Studies?have shown?that once-daily eye drops latanoprost was as or more effective as eye drops containing timolol?for treating?intraocular hypertension , and?latanoprost?and timolol were significantly more effective in lowering intraocular pressure.
Platanoprost treatment can cause a gradual change in the color of the eyes due to the accumulation of brown pigment in the iris. This effect is harmless and occurs especially in people who have mixed eye color. In most cases, the color change is slight and sometimes not seen at all.

Labetalol is a beta-blocker used to treat high blood pressure and is given alone or in combination with diuretics. The mechanism of action of labetalol is to widen the blood vessels and slow the heartbeat in order to lower blood pressure.
Like other beta-blockers, the drug may worsen signs of congestive heart failure (CHF - congestive heart failure) and may mask low blood sugar and exacerbate asthma. Labetalol may also cause sensitivity to cold weather, so be careful to wear warm clothes Avoid exposure to cold for long periods.?

Lapatinib is a new biologic drug for the treatment of?advanced?breast cancer .
Its mechanism of action is based on inhibiting the action of the epidermal growth factor receptor protein (HER2), which is present in 25% of patients with breast cancer. The excess protein causes cells to overproduce and eventually spreads throughout the body.
Unlike?trastuzumab??, it is not about an antibody that binds to a specific antigen on the cell membrane, but about a small molecule that enters the cell membrane and acts on several receptors simultaneously with the aim of blocking the normal activity of the cell and preventing its proliferation.

Quinidine is a derivative of quinine (Quinine) extracted from the bark of the quinine tree and is a drug for the treatment of arrhythmias, this drug has been known since the twenties of the last century.
Today, this drug is used primarily to maintain a regular heartbeat in people with?atrial fibrillation?and to prevent arrhythmias in the heart's ventricles.
Like many medicines used to treat a fast heart rate, the main side effect of the drug is the possibility of the drug itself to cause serious heart rate problems, that is, to increase the rate of the heart.
The use of this medicine is less today, as other medicines are used that give the same therapeutic effect, but with fewer side effects.

Ketoconazole is an effective?antifungal??drug that is used to treat fungal infections only when another effective antifungal drug is not available or cannot be tolerated and the benefits outweigh the potential risks.
Ketoconazole may also be used to treat rare fungal diseases, such as blastomycosis, histoplasmosis, and Paracoccidioidomycosis.
This medication is also used topically for fungal skin infections, such as athlete's foot, ringworm, ringworm, and dandruff.
Ketoconazole should not be given if hepatic impairment is present.

Ketotifen is an ancient antihistamine that reduces the effect of histamine in the body and is responsible for allergy symptoms that include sneezing, itching, watery eyes and runny nose.
It is mainly used to relieve itchy eyes caused by? allergic?conjunctivitis??or allergy to dust, pollen and other allergens. It is given as an eye drop for adults and children over 3 years.
It may also be used as an adjunct in the chronic treatment of mild atopic asthma in children, and since this medication is intended as a preventive treatment for asthma, it is not effective against severe asthma attacks, and other preparations should be used in these cases.

Ketamine is a drug currently used primarily in veterinary medicine and for pediatric and field anesthetics, and is sometimes used to initiate anesthesia before other general anesthetics are administered.
The drug does not relax the muscles, so if muscle relaxation is needed in addition to anesthesia, ketamine must be combined with other drugs to relax the muscles and provide support for the respiratory system by artificial respiration.
The mechanism of the effect of ketamine is to close the receptors in the brain cells that are involved in the process of learning and remembering. Therefore, ketamine leads to inhibition of brain activity, disruption of memory, a feeling of detachment from the environment and pain relief. For this reason, ketamine has also become a popular party drug in recent years.
Upon awakening from anesthesia, severe side effects may appear, such as: hallucinations, a feeling of being outside the body, anxiety, and fear. These effects and phenomena can be controlled by giving ketamine combined with a drug from the benzodiazepine family.

Quetiapine is an anticonvulsant drug of unknown etiology used to treat?schizophrenia?, manic episodes of bipolar disorder, and depression.
The efficacy of quetiapine in treating the symptoms of schizophrenia is similar to that of haloperidol, except that it causes fewer side effects, especially those that affect movement, such as Parkinsonism, and does not cause a sharp rise in the proportion of the hormone prolactin (Prolactin hormone), which makes its symptoms less Leakage of breast milk and the disappearance of menstruation.

Colistimethate sodium is an antibiotic used to treat infections caused by a variety of Gram-negative bacteria including urinary tract infections, such as cystitis and urethritis, and to treat wounds or burns and to treat infections in cystic fibrosis patients.
Temporary nervous disorders may appear during the treatment period, such as: feeling numb in the extremities, itching, dizziness, and slowness in speaking. The drug may also harm the function of the kidneys;?Therefore, the performance of the kidneys must be carefully monitored.

Colestipol belongs to a class of drugs known as bile acid sequestrants. It binds to bile acids that bind to LDL cholesterol in the intestines and form a compound that is removed from the body with the stool.
Therefore, it is used to reduce the level of harmful?cholesterol??in the blood, which is also called low-density lipoprotein (LDL) cholesterol in people who suffer from high cholesterol, which contributes to the prevention of heart disease and atherosclerosis.

Cholestyramine is a resin that binds with bile acids to form a complex compound that is excreted in the faeces.
The effect of the drug on bile acids increases stool volume and leads to an anti-diarrheal effect, and the effect of the drug in lowering cholesterol helps people who suffer from a high level of fats in the blood, and who did not respond to diet therapy or for people who are at risk of heart disease as a result of diabetes or the presence of deaths In the family as a result of a heart attack.
Sometimes medicine is given to treat diarrhea after a terminal ileectomy, as occurs in?Crohn's disease?.
Taking cholestyramine in large doses can cause bloating, mild nausea, and constipation. Cholestyramine can harm the body's ability to absorb fats and some fat-soluble vitamins.?This results in light-colored, large and foul-smelling stools, as well as vitamin deficiencies.

Colchicine is a class of anti-gout medications that affects the way the body responds to uric acid crystals, reducing swelling and pain.
Colchicine is used to prevent??acute attacks of?gout and relieve joint pain and inflammation in cases of exacerbation of gout, as the efficacy of the drug is when it is taken at the onset of symptoms directly.
Colchicine is also used to treat familial Mediterranean fever, an inherited condition that causes episodes of fever, pain, and swelling of the stomach, lungs, and joints area in adults and children 4 years of age and older.

Codeine is an opioid that is often used to relieve mild to moderate pain.
Codeine's mechanism of action is by changing the way the brain and nervous system respond to pain, resulting in less pain for certain periods of time.
In addition, it may be used to treat some other problems, such as: coughing, as it works to inhibit the part of the brain responsible for coughing.

Co-Trimoxazole is a two-component anti-bacterial drug, trimethoprim and sulfamethoxazole, which are folate antagonists.
Co-trimoxazole belongs to a class of medicines called sulfonamides.
The drug is commonly used to treat some types of bacterial infections, such as:
Pneumocystis carinii pneumonia.
bronchitis.
Urinary tract infections.
Gastrointestinal infections.
ear infections;

Copolymer-1?is a newly produced drug?used to treat multiple sclerosis.
Multiple sclerosis?is?a chronic disease of the central nervous system.?The most important symptoms of the disease are disturbances in vision, senses, movement, etc.
Today, MS is thought to be an "autoimmune" disease in which the immune system damages the myelin layer, the layer that covers nerve fibres.
The researchers believe that copolymer-1 inhibits the inflammatory process that occurs as a result of the work of the immune system, thus reducing the damage to the myelin layer and the severity of symptoms of the disease.?The long-term effects are not yet known.
It is worth noting that copolymer-1 does not treat the underlying disease, so you should not stop taking the drug without consulting your doctor, because symptoms may reappear.

Clindamycin is a lincosamide antibiotic that inhibits the growth of bacteria.
Clindamycin is used to treat certain types of bacterial infections, including infections of the lungs, skin, blood, bones, joints, female reproductive organs, and internal organs.
It is also used as a vaginal cream or suppository to treat women suffering from bacterial vaginosis and is used topically to treat??acne?.

Clonidine is a drug that belongs to a group of centrally acting alpha-agonists that lower blood pressure and act on the central nervous system.
It is used to treat?high blood pressure??by lowering the heart rate and widening the blood vessels so that blood can flow more easily through the body.
Clonidine may also be used to treat attention deficit hyperactivity disorder (ADHD) in children by affecting the part of the brain that controls attention and impulsivity.
Plus, it may help reduce flare-ups and redness associated with menopause.

Clonazepam belongs to a group of medicines known as benzodiazepines that are primarily used to treat?anxiety??and?insomnia?.
Clonazepam is used alone or in combination with other medications to control certain types of seizures in adults and children, including Lennox-Gastaut syndrome, akinetic seizures, and myoclonic seizures.
Clonazepam is also used to treat panic attacks and panic disorder, including agoraphobia, in adults.

Cloxacillin is a semi-?synthetic penicillin?antibiotic that is particularly effective against Staphylococcus aureus.
In addition to its effectiveness against infections caused by Streptococcus and Pneumococcus.
It is used to treat some types of bacterial infections, including the following:
endocarditis;
Pneumonia.
Bone and joint infections Skin infections.
Septicemia caused by susceptible strains of penicillinase-producing staphylococci.
Because this antibiotic belongs to the penicillin family, people who are allergic to penicillin are also allergic to cloxacillin.
It is worth noting that this drug is not approved in many countries, including the United States.

Clofarabine is a chemotherapy drug that belongs to the group of antimetabolites. It is an analogue of a purine nucleoside that interferes in the process of building cancer cells and their growth, thus limiting the development of cancer.
Clofarabine is used to treat?acute lymphoblastic leukemia?(ALL) in patients aged 1 to 21 years who have experienced relapse or treatment failure after at least two previous treatments.

Chloroquine is used to prevent and treat malaria. When this drug is taken orally, the drug is quickly absorbed and eliminates the disease within three days. As a precaution when going to an endemic area, the drug is given in a reduced dose.
Common side effects include: nausea, headache, diarrhea, abdominal cramps, and sometimes a rash. One of the most serious effects of chloroquine is its ability to damage the retina when taken continuously.
Chlorothiazide is a group of diuretics that remove excess fluid from the body and reduce edema in people with congestive?heart?failure, kidney disease, or cirrhosis of the liver. Chlorothiazide reduces the amount of calcium in the urine.?Therefore, it is sometimes used to prevent certain types of kidney stones.
Chlorothiazide causes the loss of potassium in the urine, which increases the risk of muscle weakness and arrhythmia, especially in patients taking digoxin to treat heart failure.?Therefore, potassium supplements are often added during treatment with chlorothiazide.

Chlorhexidine is an antiseptic and antibacterial substance that works against many germs and fungi.
It is found in many products for external use to disinfect the skin and prevent infections that may be caused by surgery, injections, or skin wounds.
It is also found in oral preparations for??gingivitis??and oral cavity disinfection, and as an adjuvant treatment for periodontitis before dental treatments to reduce gum pocket depth.

Chlorpheniramine is an antihistamine used to treat allergic conditions such as hay fever, allergic conjunctivitis, and urticaria.
Chlorpheniramine, like other antihistamines, relieves sensory symptoms in the skin such as itching, swelling and redness, in addition to alleviating colds, sneezing and itching in the eyes. It also has minor anticholinergic effects that reduce phlegm secretion.

Chlordiazepoxide/clidinium bromide is one of the compounds that are used to treat some digestive disorders, such as: gastric ulcers and?symptoms of irritable bowel syndrome?(IBS), and it also helps relieve anxiety (Anxiolytic).
Clidinium bromide has antispasmodic activity, as it reduces gastric acid secretion, while chlordiazepoxide is a central nervous system depressant (CNS), which works to relieve stress and excessive anxiety.
Taking such medicines may cause a kind of dependency, so it is necessary to avoid abrupt discontinuation of treatment so as not to cause serious side effects.
Taking this medication can cause many major side effects, such as:??dry mouth?, constipation, difficulty passing urine, drowsiness, decreased alertness, confusion, weakness, loss of balance, dizziness, and depression.

Chlorthalidone is a thiazide diuretic.
The drug removes the excess water in the body and reduces fluid retention (Edema) in people with abundant?heart failure?, kidney disease, and cirrhosis of the liver.
Chlorthalidone is often used to treat?high blood pressure?, and because this medicine reduces the amount of calcium in the urine it is sometimes used to prevent certain types of kidney stones.
Chlorthalidone is more permanent than the rest of the group, but this medicine increases the loss of potassium and other salts in the urine.

Chlorpromazine is an antipsychotic drug known since the beginning of the fifties in the last century.
Chlorpromazine is primarily used to treat the symptoms of??schizophrenia?, mania, and other conditions associated with severe, aggressive conduct disorders that need to be calmed.
Another use of chlorpromazine is used to treat nausea and vomiting, especially those caused by drug or radiotherapy, or as a result of general anesthesia for surgery.

Chlorpropamide is an oral medication for? type 2?diabetes??.
The drug lowers blood sugar levels by stimulating the secretion of the hormone insulin from the pancreas and stimulating the entry of sugar into the cells of the body.
Of all the oral diabetes medications, chlorpropamide has the longest lasting effect.
Caution should be exercised when using the drug because it can accumulate in the body and cause a sharp drop in blood sugar levels.

Chloramphenicol is an antibiotic found in many preparations for the topical treatment of eye and ear infections.
Although most people experience almost no side effects from this drug, chloramphenicol in rare cases leads to bone marrow suppression and a severe deficiency of blood cells that can cause death.?That's why chloramphenicol is used orally or by injection only in severe infections that do not respond to other safer medicines.

Clorazepate is a drug in the benzodiazepines family of medicines that works by decreasing abnormal electrical activity in the brain.
It is used as a short-term treatment to relieve anxiety and tension, and is also used to treat withdrawal symptoms caused by quitting alcoholism, and to help treat certain types of??epileptic seizures?.
The use of clorazepate may lead to getting used to its use when taken for a continuous period on a regular basis, and its pharmacological efficacy decreases with the passage of time.
When the use of clorazepate is stopped for a while or it is replaced by another type of medicine, the desired effect of clorazepate may return when it is used again.?

Caldronate belongs to the group of bisphosphonates and is used to treat?hypercalcemia?caused by tumors.
Caldronate may also be used in the treatment of?Paget's disease?, which leads to the development of deformed bones.

Clotiapine is an atypical antipsychotic drug used to treat acute or chronic?schizophrenia?, and it may help treat acute anxiety, irritability, and agitation in non-psychotic disorders.
It is worth noting that this drug is not approved in the United States and Canada.

Clopidogrel is a drug that prevents blood clots from forming and reduces the risk of myocardial infarction or?stroke?in patients who have had it before.
Clopidogrel is an effective drug in preventing stent-related thromboembolism in people with coronary artery disease.

Clobetasone butyrate belongs to the group of corticosteroids, and is used to treat eczema and other different types of skin infections, such as: atopic dermatitis, otitis externa, and rashes caused by otitis externa. Diapers, and insect stings.?
Excessive use of clobetazone, as with other corticosteroid treatments, leads to permanent loosening of the skin, and the risk is especially high when treating children and when applying lotions to the face or large areas of the skin.?

Clobetasol propionate, which belongs to the group of corticosteroids, is highly effective.
Clobetasol is suitable for the short-term treatment of skin infections such as: psoriasis, eczema that does not respond to other treatments, lichen planus, and other skin infections that do not respond to less potent corticosteroids.
Excessive use of clobetazole, like other corticosteroids, leads to permanent loosening of the skin, and the risk is greater when treating children with clobetazole or when applying to the face or large areas of the skin.

Clobazam is a medicine belonging to the family of benzodiazepines that works by decreasing abnormal electrical activity in the brain.
It is used with other medications to control seizures in adults and children 2 years of age and older who have Lennox-gastaut syndrome, a severe form of pediatric epilepsy that causes developmental and behavioral problems.
As with other benzodiazepines, clobazam may cause addiction to the patient if it is taken for a long period of time or in relatively high doses, so it is forbidden to take this drug in frequent or continuous periods without consulting the doctor.
It is also worth noting that this medicine may cause suicidal thoughts in some patients, so inform your doctor immediately if you notice any changes in mood or symptoms.

Clarithromycin is a macrolides antibiotic that works by inhibiting the growth of bacteria.
Clarithromycin is effective in treating mild to moderate infections caused by bacteria sensitive to these antibiotics.
Clarithromycin is usually used to treat the following conditions:?
Sinusitis?.
Inflammation of the middle ear.
Pneumonia?.
bronchitis.
Skin infection.
Sore throat and tonsillitis.
Stomach ulcers caused by Helicobacter pylori when used with other medicines.
Mycobacterium Avium infection in AIDS patients.

Cladribine is a chemotherapy drug given to treat hairy cell leukemia, and in rare cases it is used to treat chronic lymphoid leukemia - CLL or non-Hodgkin's lymphoma.
Cladribine causes damage to the genetic material of cancer cells, preventing these cells from growing and dividing, which leads to their death.
As with other anti-cancer drugs, cladribine impairs the production of various blood cells in the bone marrow, causing anemia, a higher risk of infections and abnormal bleeding. Cladribine may also cause changes in the functioning of the liver and kidneys, elevated levels of uric acid, and neurological symptoms. Such as loss of sensation in the arms or legs.

Sodium Cromoglycate is a medicine used to prevent??asthma?attacks and other allergic conditions.
Sodium comoglicate can also be used as eye drops to prevent allergic conjunctivitis, nasal drops to prevent allergic rhinitis, and the drug can be taken in capsules to treat allergic gastrointestinal tract.

Crotamiton is?one of the medications used to treat itchy skin, including itching caused by?scabies?. Its mechanism of action is to kill the mites that cause scabies. It also relieves itching caused by scabies and other skin diseases.
The treatment should be placed on the skin only, with the need to avoid applying it to the mouth, eyes, vagina and any inflamed skin area.
Calcium carbonate is an antacid that removes stomach acid, and therefore is used to relieve heartburn,?peptic ulcers?, and gastroesophageal reflux. Calcium carbonate is also used as a nutritional supplement in people who suffer from low calcium levels in the stomach.?the blood.
Common side effects of calcium carbonate mainly include: constipation, headache, and when taken in large doses can lead to the formation of kidney stones and may cause nausea and vomiting.

Carbocisteine ??is a mucolytic drug that works by making??phlegm??less thick and sticky, making it easier to cough up.
It is used as an adjunctive treatment to dissolve phlegm in respiratory disorders that cause excessively sticky mucus production, such as:??chronic obstructive pulmonary disease??(COPD) and cystic fibrosis.

Glucosamine sulfate is used to treat symptoms of?osteoarthritis?.?Initial treatment with glucosamine sulfate, with the onset of the early stages of the disease, can protect the cartilage in the joints, relieve pain, and lead to an improvement in performance and quality of life.
The preparation is in the form of a powder that combines the active substance, glucosamine sulfate together with sodium ions, to form a salt together, which helps to give the preparation a better stability, allowing the delivery of the active substance to the joints in a high concentration.
Arthryl complies with registration standards in many European countries and has been shown to be effective and safe in clinical research.?Therefore, glucosamine is the only registered as a prescription drug, as the rest of the recognized glucosamine products are registered as food additives, without a prescription.
It is acceptable to use glucosamine sulfate with?NSAIDs?, especially during the first two weeks of treatment.

Polymyxin B sulfate is an antibiotic belonging to the polymyxins family, and is used to treat various types of infections, such as: urinary tract infections, eye infections, and ear infections, in addition to meningitis caused by bacteria sensitive to this type of antibiotic.
Polymyxin B sulfate is combined in most preparations with other antibiotics.
Although the side effects of polymyxin B sulfate are rare, it can poison the nervous system and cause symptoms such as: anxiety, dizziness, and shortness of breath. In rare cases, this drug may cause kidney damage.

Candesartan is an angiotensin II receptor blocker medication.
Angiotensin II is a substance in the body that encourages the contraction of blood vessels, so blocking its effectiveness causes blood vessels to widen, blood flowing smoothly, and blood pressure lowering.
Candesartan is used to treat high blood pressure in adults and children who are at least 1 year old, and to treat congestive heart failure.
This type of medicine is used to treat patients who cannot tolerate the effects of medicines from the family of ACE inhibitors, such as: Captopril, because of the side effects they cause, such as coughing or?angioedema?

Cannabidiol and THC are two active substances extracted from the cannabis plant that have been combined into a prescription drug used to treat cancer patients who experience pain despite taking analgesics and to treat multiple sclerosis patients with neuropathic pain or muscle stiffness.
This medicine is distinguished from other medicines equivalent to it from its group in the combination of both active substances, which greatly reduces the side effects.?
At the beginning of treatment, tachycardia and orthostatic hypotension may occur, i.e. when moving from a lying position to a sitting position, so this medication is not recommended for people who suffer from irregular heartbeat.

Calcitonin is a hormone secreted by the thyroid gland, which reduces the loss of calcium from the bones and helps maintain healthy levels of calcium in the blood.
The synthetic preparation of calcitonin is used to treat?osteoporosis?, Paget's disease, and high blood calcium.

Calcipotriol is a drug that is chemically similar to vitamin A and is designed for external use in the treatment of mild to moderate psoriasis. Calcipotriol slows down rapid cell division, leads to normal cell division and improves the appearance of the skin.
Use as a contraindication for patients with calcium metabolism disorders Not intended for use on the face and hands should be washed thoroughly after use unless psoriasis is present on the hands.

Caspofungin is an antifungal drug that belongs to the family of medicines known as echinocandins. Its mechanism of action is by inhibiting the production of the fungal cell wall, preventing the growth of the infection-causing fungi.
Carvedilol is a beta-blocker that dilates blood vessels and treats high?blood pressure?.
Carvedilol may also be used to treat heart failure.
Sometimes carvedilol is given with other medicines, such as diuretics.

Carbidopa belongs to the class of decarboxylase inhibitors and is used with another medicine called??levodopa??to treat symptoms of Parkinson's disease caused by a lack of dopamine in the brain.
It is also used to treat muscle symptoms similar to Parkinson's disease caused by certain medications, or caused by encephalitis, or injury to the nervous system due to carbon monoxide or manganese poisoning.
When levodopa is given alone it is broken down in the body, and only a small portion of the substance reaches the brain tissue, so carbidopa works by preventing the breakdown of levodopa before it reaches the brain.
Then levodopa can be taken in lower doses, which contributes to reducing its side effects, such as: nausea and vomiting, and it is worth noting that carbidopa has no effect when used alone.

Carbomer is one of the chemical compounds that are manufactured from acrylic acid. Carbomer is used as the main compound in?artificial tears substitute?. It is available in the form of a gel-like liquid used to moisturize the eyes and relieve symptoms of dryness in them.
This gel is used less often compared to eye drops, due to its high viscosity, which gives a longer treatment effect. It is also forbidden to use the gel when soft?contact lenses?are present , and before putting the lenses back in, you must wait at least 30 minutes after applying the gel.
Carbomer can also be used in emulsions to give them the right viscosity, so they are used in most cases as inactive substances.

Carbamazepine belongs to a class of medications called anticonvulsants, and it works by decreasing abnormal electrical activity in the brain.

Carbaryl is a cholinesterase inhibitor used to treat???head and pubic?lice .
It is worth noting that it is not recommended to use this drug for scabies.

Capecitabine is an anti-cancer that works to treat the following conditions: large bowel and rectal cancer in its advanced stages and after a tumor removal operation, and for the treatment of breast cancer in its advanced stages or that has spread to other places, where it is given after previous chemotherapy attempts failed in addition to Docetaxel. (Docetaxel) or on its own.
Fluorouracil, which is produced by the lysis of the drug, causes the death of cancer cells by controlling the genetic engineering structure of those cells. Because of the conversion of the drug to fluorouracil, especially in cancer cells, its effect on healthy cells is less compared to the traditional treatment with fluorouracil that is administered by injection.
Unlike other anti-cancer drugs, it is not uncommon for the drug to lead to hair loss or to inhibit bone marrow cells.

Cabergoline is a drug that directly stimulates dopamine receptors in the brain and reduces the production of the hormone prolactin.
Cabergoline is used in the treatment of Parkinson's disease, and in the treatment of cases in which there is an increased production of prolactin, such as: disturbances or amenorrhea, increased secretion of milk from the breasts, lack of ovulation, and the presence of tumors that lead to the secretion of prolactin, in addition, cabergoline works to impede Or prevent the secretion of milk in women after childbirth when the inability or lack of desire to breastfeed.
For the treatment of Parkinson's disease, cabergoline can be given with carbidopa and levodopa.

Capsaicin is a natural substance extracted from hot peppers and is found in various topical preparations for pain relief by affecting the nerve cells in the skin responsible for pain, which leads to a decrease in the activity of these neurons and reduces the feeling of pain.
As a result of the activity of capsaicin, nerve irritation occurs in the tissues, which leads to a local feeling of heat and burning at the beginning of use, but with time and regular use, the drug contributes to reducing the amount of the substance responsible for feeling pain.

Captopril is a medicine used to treat??high blood pressure and?is one of a group of medicines called angiotensin-converting enzyme (ACE) inhibitors.
As with many other medicines that lower high blood pressure levels, captopril dilates blood vessels and facilitates blood flow.
Captopril can be given to patients after a myocardial infarction in order to reduce the pressure on the heart and improve its performance, and it may also be used to protect the kidneys in case of diabetic nephropathy

Cabazitaxel is a chemotherapy drug that is used to treat advanced prostate cancer, as the drug prevents the growth and division of cancer cells, leading to their death.
Like other anticancer drugs, the drug suppresses the production of different blood cells in the bone marrow, which causes anemia and increases the risk of infections and abnormal bleeding.

Phenylephrine is a decongestant medication widely used to reduce nasal congestion.
Phenylephrine is used in many topical preparations to relieve symptoms of hay fever and colds. Although it is less effective than other decongestants, it works longer with fewer side effects.
Small doses of this medicine can reduce the burning in the eye in?conjunctivitis??by contracting the muscles of the blood vessels in the eye membrane

Phenelzine belongs to the class of monoamine oxidase inhibitors (MAOIs) that increase the level of serotonin, norepinephrine, and dopamine in the brain.
The use of phenelzine was reduced after the development of several other drugs with side effects, and it is now used to treat symptoms of atypical depression or neurotic depression in adults who have not responded to other medications.
It is worth noting that phenelzine is not used to treat major depression, bipolar disorder, or what is known as bipolar disorder.

Phenylpropanolamine is a?decongestant?medication .
Phenylpropanolamine is available as an ingredient in many cold medicines and can be obtained without a doctor's prescription.
Phenylpropanolamine relieves inflammation and swelling in the blood vessels in the nose, thus relieving nasal congestion in case of the common cold, Hay Fever, and Sinusitis.

Phenytoin is a drug widely used for the long-term treatment of many types of??epilepsy?.
Phenytoin reduces the risk of convulsions by reducing electrical discharges in the brain.

Phenolphthalein is a class of stimulating laxatives that causes the intestines to contract and move more, and is suitable for limited use in the treatment of diarrhea that other treatments have failed to treat or when urgent action is required.
Phenolphthalein was previously sold without a prescription, but after it was shown to cause cancer in laboratory animals when given in very high doses, it is now sold by prescription only.

Phenoxybenzamine is an alpha receptor blocker.
This medicine is used to reduce high blood pressure that occurs in cases of pheochromocytoma, which is an enlargement of the adrenal gland that leads to increased secretion of hormones that cause a marked increase in blood pressure, and it is also used to treat benign tumors that affect the?prostate?

Vinorelbine is a chemotherapy drug used to treat non-small cell lung cancer,?advanced?breast cancer , and prostate cancer.
Vinorelbine belongs to the family of chemical medicines called plant alkaloids that are extracted from plants.
This medication prevents cancer cells from dividing, causing them to die.
This medicine is contraindicated in patients who require long-term oxygen therapy, and during radiotherapy, if the liver is part of the treated area.
Like all other anti-cancer drugs, phenorlepine inhibits the production of various blood cells in the bone marrow, which leads to?anemia?, susceptibility to infections, and the occurrence of abnormal bleeding.

Phenobarbital has been in use for more than 70 years and belongs to a group of medicines called barbiturates, and it works by slowing down the activity of the brain and nervous system.

Fenfluramine is a medication used to treat seizures caused by Dravet syndrome and is used by adults and children over the age of two.
The use of the drug may cause poor appetite and weight loss, but it is not used to treat?obesity?without a problem of epilepsy.

Vincristine is an effective anti-cancer substance, used to treat many malignant tumors, and it is usually given with other drugs.
Vincristine is used to treat the following conditions:
Acute leukemia?.
Malignant lymphoma cancers.
?Small cell lung cancer?(Small cell carcinoma).
?Breast cancer?.
Brain tumors treatment.??
Like other anti-cancer drugs, vincristine inhibits the formation of various blood cells in the bone marrow, which leads to anemia and makes the patient more susceptible to infections and abnormal bleeding.
Other side effects include constipation, hair loss, nerve disorders, and in rare cases, seizures

Finasteride is a drug that blocks the conversion of male testosterone to Dihydrotestosterone.
Finasteride is used to treat symptoms of benign prostatic hyperplasia. Finasteride reduces the size of the??prostate??and thus improves urine flow.
Finasteride is also used to treat androgenic alopecia, as it has been shown to be effective in treating mild to moderate alopecia.

Phenazopyridine is a drug that is excreted in the urine and is used to relieve pain, burning, or persistent urination caused by irritation of the bladder membrane due to infection, surgery or endoscopic examination.
Phenazopyridine does not treat the inflammation itself, only its symptoms.?Therefore, the procedure in cases of infection is a treatment that combines phenazopyridine and an antibiotic to treat the infection itself.
Among the common side effects that do not cause concern for this drug: red-orange coloring of urine and coloring of contact lenses in the eyes, so it is recommended to refrain from wearing contact lenses during the use of the drug.

Felodipine is a drug that belongs to a group of drugs called calcium channel blockers. Calcium is necessary to constrict blood vessels, blocking the passage of calcium, dilating blood vessels and lowering blood pressure.
This medicine is mainly used to treat patients with high blood pressure, as lowering blood pressure can help reduce the risk of a stroke or heart attack.
It may be used in some cases to treat angina pectoris.

Filgrastim is a drug that stimulates the production?of white blood cells?called neutrophils.
The drug works similar to a protein in the body called granulocyte colony stimulating factor, which helps produce neutrophils.

Vildagliptin is a drug intended for the treatment? of type 2?diabetes mellitus??that belongs to the enzyme dipeptidyl peptidase-4 (DPP-4) inhibitors that break down incretin hormones.
When this enzyme is inhibited, the drug succeeds in increasing the level of incretin that affects the pancreas to increase the production and secretion of insulin and reduce the production of glucagon, thus helping to balance and regulate blood sugar levels.
?Your doctor may recommend vildagliptin along with other medications to treat diabetes if one medication isn't enough to balance your blood sugar. However, it's important to continue diet and exercise, as well as medication.

Fexofenadine is an antihistamine used to treat allergic rhinitis and allergic skin conditions such as urticaria.
Fexofenadine is a metabolite that is the active metabolite of another antihistamine drug known as terfenadine. Fexofenadine has no depressant effect on the nervous system;?Therefore, it does not cause fatigue, but unlike terfenadine, it does not cause?arrhythmias?and does not interact with other medications.

Verapamil belongs to a group of medicines called calcium channel blockers, which play a role in the transmission of signals in the muscles of the heart and blood vessels.
Verapamil is used to treat the following conditions:
high blood?pressure
Arrhythmias.
Angina pectoris.
Verapamil reduces the frequency of?angina?attacks , but unlike other calcium channel blockers it does not work fast enough to relieve pain in an advanced attack. .
Verapamil is given because of its effect on the heart to treat certain types of arrhythmias. For this purpose, the medicine is given by injection into a vein or in the form of tablets. Verapamil is not usually given to people who suffer from the following conditions:
Low blood pressure.
Bradycardia.
heart failure
This is because verapamil exacerbates these conditions.

Vigabatrin is an anticonvulsant drug that is given together with other anticonvulsant drugs to patients with epilepsy who do not respond adequately to treatment.
The mechanism of effect of Vigabitrin is the selective inhibition of the enzyme responsible for dismantling and degrading the neurotransmitter called Gamma-Aminobutyric Acid / GABA, which leads to an increase in its levels in the brain, thus increasing the inhibitory effect of neuronal activity in the brain.
This medicine should not be given to patients who have suffered from psychosis or behavioral disorders in the past.
The main side effects of vigabitrin include: vision impairment, reduced visual fields, and weight gain.

Fulvestrant is a medicine intended to treat end -stage?breast cancer??in postmenopausal women.
Fulvestrant binds to estrogen receptors on breast cancer cells and makes them less active. In addition, by decreasing the concentration of these receptors, this mechanism of action impairs cancer cell division.
Fulvestrant is given to women whose disease has come back or has progressed despite receiving anti-estrogen therapy with medicines such as tamoxifen or anastrozole.
Most patients tolerate fulvestrant well.

Fosinopril is a drug that belongs to a class of medications called angiotensin-converting enzyme (ACE) inhibitors. It works by decreasing certain chemicals that cause blood vessels to constrict, resulting in smoother, more efficient blood flow.
Fosinopril is used in the treatment?of high blood pressure?and heart failure, and most patients accept the treatment well, but before starting the use of the drug, it is necessary to ascertain the integrity of kidney function.?
The main side effects of this drug are coughing, dizziness, and nausea, and it may cause a drop in blood pressure when moving from a lying position to standing, which may lead to dizziness, confusion, or loss of consciousness.

Sodium phosphate belongs to osmotic laxatives. It contains the laxative salts of sodium phosphate monobasic monohydrate and sodium phosphate dibasic anhydrous.
This saline laxative is thought to work by increasing fluid in the small intestine, so it is primarily used to empty the intestines before colonoscopy, surgeries, or X-ray examinations of the intestine.
This medication can also be used to relieve occasional constipation, but other, somewhat milder types of laxatives are preferred when treating constipation whenever possible.

Fosamprenavir is a medicine intended for the treatment of people with HIV, which causes AIDS. It belongs to the class of protease inhibitors.
This enzyme plays a central role in the replication and maturation of the virus, and its inhibition enables this process to be suppressed, thus reducing the amount of HIV in the blood.
It is worth noting that it does not cure this virus, but it may reduce the chance of developing acquired immunodeficiency syndrome, or?AIDS?, and ?diseases associated with HIV, such as infection and cancer.

Voriconazole is a medicine intended for the treatment of acute fungal infections, such as: Aspergillosis, Scedosporium, Fusarium, and infections that were resistant to previous treatment with Fluconazole.
These infections mainly affect people with low immunity, such as AIDS patients, cancer patients who receive chemotherapy, and?organ transplant?recipients , and can be life-threatening for them.
Voriconazole acts like other drugs of its family, such as: fluconazole and itraconazole, by blocking the building of the fungus cell wall.
Voriconazole can cause liver damage, so liver tests are needed during treatment. Increased liver enzymes usually resolve with a change in the dose, or the drug is stopped.
The doctor must be informed of the following symptoms that may indicate a deterioration in the functioning of the liver:?yellowing of the skin?or eyes, persistent itching, loss of appetite, fatigue and weakness, frequent nausea and vomiting.

Furosemide is a fast-acting, effective loop diuretic that has been in use for more than twenty years. It works by causing the kidneys to remove excess water and salt from the body into the urine.
Furosemide, like other diuretics, is mainly used to treat fluid retention in body tissues or edema caused by?heart failure??,?pulmonary edema,?and liver and kidney disease. Furosemide is also used to treat high blood pressure. ?
Furosemide is particularly effective in treating people with impaired kidney function who do not respond well to thiazide diuretics.
Furosemide may increase potassium loss, which may result in a wide range of side effects, which is why furosemide is often combined with potassium supplements or potassium-sparing diuretics.

Formoterol?is a long-acting medication used to dilate the bronchi. Its mechanism of action depends on relaxing the muscles surrounding the bronchi.
Formoterol is mainly used to treat?asthma?, as it relieves symptoms and reduces the possibility of attacks, knowing that it is not used during an attack. As for the treatment of acute asthma attacks, a short-term effective bronchodilator should be used, such as Salbutamol. .
Formoterol is not a substitute for inhaled steroids, so they can be used together, as many attempts to combine the two treatments in one inhaler have shown greater benefit and efficacy than using them alone.
Formoterol is one of the appropriate medications for most patients, but in the event of any side effects of treatment, it is preferable to consult a doctor to take the appropriate action, and you should not take an extra dose of what the doctor recommended.

Phentermine is a drug used to help treat severe?obesity?associated with other problems, such as high blood pressure, diabetes, and hyperlipidemia.
Phentermine is similar in its action to amphetamine, in that it stimulates the central nervous system, which leads to a decrease in appetite. It is important to know that the treatment is only used for a few weeks, as it can cause long-term side effects such as addiction.?
Taking the treatment may cause many side effects, such as: nervousness, head pain, dizziness, trembling, insomnia, dryness or bad taste in the mouth, digestive disorders, in addition to??high blood pressure??and irregular heartbeat.

Fentanyl belongs to the narcotic or opiate family of pain relievers and is available in several ways, and it works by changing the way the brain and nervous system respond to pain.
Oral fentanyl is used to treat sudden attacks of pain in cancer patients who regularly take opioid pain relievers and no longer have an effect as their bodies adapt to them.
Also, transdermal patch therapy aims to relieve moderate to severe chronic pain, which does not respond to other opioid pain relievers.
But unlike the oral or dermal fentanyl methods, the injection is intended for short-term pain relief, such as: surgery pain, in addition to its use in general anesthesia.
Long-term use of fentanyl, as is the case with other opioid analgesics, can lead to dependence and addiction of the patient to the analgesic. However, short-term consumption will not cause dependence on treatment, and it is possible to stop using it without difficulties.

Flecainide is a drug used to treat arrhythmias, to treat ventricular arrhythmias, and to maintain a normal heart rate in patients with ventricular fibrillation and ventricular flutter.
Because of the side effects of this medicine, it is used only in cases of unresponsiveness to other medicines in patients with severe and dangerous arrhythmias.
Like other drugs from this family, flecainide can cause very serious arrhythmias, and it can cause an inhibition of electrical conduction in the heart, which leads to a very slow heartbeat.
Since flecainide can depress myocardial action, it should not be given to patients with congestive heart failure or to people who have had a previous myocardial infarction.

Flunitrazepam belongs to a group of medicines called benzodiazepines that have a depressant effect on the central nervous system, and are used to calm, relax muscles, and even put them to sleep.
Its primary use is as a short-term treatment for severe insomnia that does not respond to treatment with other hypnotic drugs.
In comparison with other benzodiazepines, flunitrazepam was found to be the most addictive, and some people even used it in a bad way as a type of drug that helps rape, causing hallucinations and sleep and impairing memory.

Fluconazole is an antifungal medicine that belongs to a class of medicines called triazoles. It works by slowing the growth of the fungi that cause infection.

Fluoxetine is an antidepressant that belongs to a class of drugs called selective serotonin reuptake inhibitors (SSRIs), which work by inhibiting the reuptake of serotonin by nerve cells, thus increasing its level in the brain.

Fluphenazine belongs to a group of medicines called phenothiazine antipsychotics.
These drugs are used to treat psychotic disorders, such as schizophrenia, and to relieve associated psychotic symptoms, such as hallucinations, delusions, and aggression.
This medication can be given by long-acting injection (Depot). This form of medication is particularly suitable for patients who do not remember to take the medication every day.

Fluvoxamine is an antidepressant and anxiety medication that belongs to the group of selective serotonin reuptake inhibitors (SSRIs), which inhibits the reuse and uptake of serotonin, resulting in an increase in its level in the brain.
Fluvoxamine is primarily used to treat obsessive-compulsive disorder, social anxiety disorder, or social phobia.
This medicine is not recommended for transient and fleeting states of depression and nervousness.

Fluvastatin belongs to the family of statins and is used to lower the level of?cholesterol?in the blood.
The mechanism of action of Vulvastatin depends on the inhibition of the activity of the enzyme responsible for the production of cholesterol in the liver, which leads to a decrease in the level of total cholesterol, a decrease in the level of triglycerides, and a decrease in the level of bad cholesterol (LDL) in the blood, as well as an increase in the level of good cholesterol ( HDL) in the blood.
Fluvastatin also improves the proper function of blood vessels by slowing their blockage.
Fluvastatin is usually well tolerated by patients' bodies, but in rare cases it may cause?liver function?disorders ?, muscle aches or weakness.

Fluocinolone is a moderately effective corticosteroid topical anti-inflammatory used to treat skin infections that respond to other corticosteroids, and to treat?psoriasis?, especially of the scalp.
Extreme caution is required when using it in children and adolescents, as its use in these generations must be accompanied by medical follow-up.
Excessive use of fluocinolone may lead to sagging skin and absorption of the drug in various parts of the body, causing unwanted side effects.

Fluorouracil is an anticancer drug that belongs to a class of drugs called antimetabolites. It works by slowing or stopping the growth of abnormally fast-growing cells such as cancer cells.
It is mainly used to treat bowel and rectal?cancer, breast?cancer ,?stomach cancer?, and?pancreatic cancer?, and fluorouracil is often given in combination with other anti-cancer drugs.
Fluorouracil is also used topically to treat actinic or solar keratoses, which cause an overgrowth of scaly skin caused by years of excessive exposure to sunlight.
It is also used topically to treat a type of??skin??cancer called superficial basal cell carcinoma.

Fluorometholone is a corticosteroid given for topical treatment of inflammatory or?allergic?eye conditions.
The advantage of fluorometholone is that it is less dangerous to increase intraocular pressure compared to other corticosteroids, such as: Dexamethasone, and the drug is well tolerated by the vast majority of patients.
Some formulations contain polyvinyl alcohol, whose function is to provide moisture, relieving dryness and discomfort in sore eyes.
Fluorometholone is contraindicated in cases of fungal infections, such as: tuberculosis in the eye (Ocular tuberculosis), and cases of viral infections.

Fludrocortisone is a synthetic corticosteroid, used in cases of decreased production of the hormone cortisol by the adrenal gland, such as:?Addison?'s disease.
Fludrocortisone also stimulates the absorption of sodium from the kidneys into the blood circulation, thus preventing the loss of sodium in the urine, so it is used to treat the salt loss that characterizes the Adrenogenital Syndrome.
Fludrocortisone weakens the body's ability to fight infection, so it is preferable to stay away from patients with tuberculosis and varicella, and not to take the vaccine made of live viruses.
It is also recommended that people receiving long-term treatment with fludrocortisone keep a treatment card with them.

Fludarabine is a chemotherapy drug used to treat chronic lymphoid leukemia (CLL) and to treat malignant non-Hodgkin's lymphoma in patients who have not responded to standard therapy or when disease progresses during or after standard therapy.
Like other anti-cancer drugs, fludarabine impairs the production of various blood cells in the bone marrow, which leads to anemia, increased susceptibility to infections and abnormal bleeding.
Giving fludarabine by intravenous injection in a large dose may lead to the emergence of neurological symptoms, such as: blindness, coma, and death.

Fluticasone is a corticosteroid medication that works by blocking the release of certain natural substances that cause symptoms of inflammation, itching, swelling and redness.

Flutamide is a hormonal anti-cancer drug used to treat prostate cancer. It can be given alone or with other drugs that reduce testosterone secretion from the testicles.
Flutamide is an anti-androgens similar in structure to testosterone, and works by blocking the binding of testosterone to receptors on the surface of prostate cancer cells. The absence of testosterone slows or stops the growth of cancer cells.
The medicine may cause life-threatening liver damage.?Therefore, the doctor should be informed immediately if symptoms occur, such as: nausea, vomiting, stomach pain, loss of appetite, fever, yellowing of the skin and eyes, dark urine, and fatigue.

Flupentixol is??one of the antipsychotics, which works by blocking dopamine receptors in the brain, which makes it used to treat many conditions, such as schizophrenia and?bipolar disorder?. Depression.?
Flupentixol is available as tablets and intramuscular injections that are used for longer periods, especially in people who have not responded well to treatment with the tablets.
Flupentixol may cause many unpleasant side effects, such as: dyskinesia, akathisia, drowsiness, blurred vision, and dry mouth.
Caution should be exercised when giving this medicine to people with certain conditions, such as: glaucoma, benign enlarged??prostate, and Parkinson's disease.

Famotidine uses include the treatment of peptic ulcers and the treatment of cases of excessive acid production in the digestive system.
Famotidine is also used to treat Zollinger-Ellison syndrome, which is characterized by increased?gastrin?secretion , which in turn leads to increased acid secretion and thus causes ulcers.

Famciclovir is an antiviral medication used to treat patients with shingles and genital herpes.
Shingles, which is caused by the herpes zoster virus, leads to the appearance of vesicular sores and a general bad feeling. An important complication of this disease is severe headache, which may last months and perhaps years in some cases.
Research shows that famciclovir may help shorten the duration of sores and pain, but famciclovir is not effective in treating herpes zoster infection and genital herpes, as there is no research to indicate the effectiveness of this drug in treating other herpes infections.
Common side effects of this drug include headaches and nausea. In addition, the treatment is well tolerated by most patients.

Valganciclovir is??an antiviral drug that is used to treat or prevent CMV infection, especially in immunocompromised patients.
In the body, valganciclovir quickly converts to ganciclovir, which is the active form of it, which leads to the accumulation of the active substance in the body more quickly compared to other medicines such as cimefene.?Therefore, the need to follow the instructions for taking the medicine increases to avoid poisoning.
It is important to know that valganciclovir causes problems in developing fetuses.?Therefore, men and women of childbearing age should use??contraception??during treatment and up to 90 days after completion of treatment.
Valganciclovir may also reduce the production of various blood cells from the bone marrow (Bone Marrow), which can lead to anemia and infection, as well as abnormal bleeding.
Valganciclovir is??an antiviral drug that is used to treat or prevent CMV infection, especially in immunocompromised patients.
In the body, valganciclovir quickly converts to ganciclovir, which is the active form of it, which leads to the accumulation of the active substance in the body more quickly compared to other medicines such as cimefene.?Therefore, the need to follow the instructions for taking the medicine increases to avoid poisoning.
It is important to know that valganciclovir causes problems in developing fetuses.?Therefore, men and women of childbearing age should use??contraception??during treatment and up to 90 days after completion of treatment.
Valganciclovir may also reduce the production of various blood cells from the bone marrow (Bone Marrow), which can lead to anemia and infection, as well as abnormal bleeding.

Valsartan belongs to the angiotensin II receptor antagonists, as it dilates blood vessels, allowing smooth blood flow.
Valsartan is used to treat??high blood pressure in??adults and children 6 years of age and older, either alone or with other medications.
A stronger anti-hypertensive effect is achieved when a low-dose diuretic is added with valsartan, and valsartan is also available in combination with hydrochlorothiazide.
Valsartan is also effective in treating heart failure and reducing the risk of death after a heart attack.
It is given to patients who cannot tolerate medicines that belong to the family of ACE inhibitors because of their side effects such as coughing or??angioedema??.
Sodium valproate is an antispasmodic medicine.
This drug works similarly to other anticonvulsant drugs, in that it reduces electrical discharges in the brain, and sodium valproate is successful when used for an extended period.

Valacyclovir is an antiviral drug used to treat patients with herpes infection. This drug speeds up the recovery from infection and relieves the pain of herpes sores and shingles.
In addition, it is used as a preventive treatment for cytomegalovirus infection in people with AIDS or in patients who have undergone organ transplantation or bone marrow transplantation, and the effect of the drug in the treatment of smallpox (Chickenpox) has been investigated.
Chemically speaking, acyclovir is derived from valacyclovir, as valacyclovir is broken down in the body to acyclovir.

Vardenafil is used to treat erectile dysfunction or impotence in men. It belongs to the class of phosphodiesterase type 5 inhibitors (PDE-5 inhibitors).
And it works by increasing blood flow to the penis during sexual stimulation and thus to the occurrence of an erection, and it is important to mention that Vardenafil, like other drugs in its group, works only when there is a sexual stimulus, it does not in itself stimulate sexual desire.
The effectiveness of Vardenafil lasts for several hours, but the continuation of an erection depends only on the continuation of the sexual stimulus, and it does not cure erectile dysfunction, nor does it work to protect the person from??sexually transmitted diseases?, nor does Vardenafil prevent pregnancy.
Vardenafil is contraindicated in people who are taking nitrate-type vasodilators such as isosorbide mononitrate, isosorbide dinitrate, and nitroglycerin.

Category

Chemical class: Soluble fusion protein, human recombinant fusion protein
Therapeutic class: Antirheumatic

Pregnancy category: C

Indications

To reduce signs and symptoms, induce major clinical response, inhibit progression of structural damage, and improve physical function in patients with moderate to severe active rheumatoid arthritis and an inadequate response to methotrexate or a tumor necrosis factor antagonist
IV: Adults weighing more than 100 kg (220 lb). Initial: 1,000 mg infused over 30 min, repeated in 2 to 4 wk. Maintenance: 1,000 mg infused over 30 min every 4 wk starting at wk 8. Adults weighing 60 to 100 kg (132 to 220 lb). Initial: 750 mg infused over 30 min, repeated in 2 to 4 wk. Maintenance: 750 mg infused over 30 min every 4 wk starting at wk 8. Adults weighing less than 60 kg. Initial: 500 mg infused over 30 min, repeated in 2 to 4 wk. Maintenance: 500 mg infused over 30 min every 4 wk starting at wk 8. To reduce signs and symptoms of moderate to severe active polyarticular juvenile idiopathic arthritis
IV: Children ages 6 to 17 weighing more than 100 kg. Initial: 1,000 mg infused over 30 min, repeated in 2 to 4 wk. Maintenance: 1,000 mg infused over 30 min every 4 wk starting at wk 8. Children ages 6 to 17 weighing 75 to 100 kg. Initial: 750 mg infused over 30 min, repeated in 2 to 4 wk. Maintenance: 750 mg infused over 30 min every 4 wk starting at wk 8. Children ages 6 to 17 weighing less than 75 kg. Initial: 10 mg/kg infused over 30 min, repeated in 2 to 4 wk. Maintenance: 10 mg/kg infused over 30 min every 4 wk starting at wk 8.

Mechanism of Action

Inhibits T-cell activation by binding to CD80 and CD86 to block interaction with CD28. CD28 is part of the co-stimulatory signal needed for full activation of T cells. Activated T cells have been implicated in the pathogenesis of rheumatoid arthritis. With decreased proliferation of T cells, inflammation and other evidence of rheumatoid arthritis decrease.

Incompatabilities

Don’t infuse abatacept solution with other in the same intravenous line concurrently because it isn’t known if the may interact.

Contraindications

Hypersensitivity to abatacept or its components immunosuppressants: Possibly increased risk of serious infection live-virus vaccines: Possibly decreased response to vaccine, and risk of infection with live virus tumor necrosis factor antagonists: Increased risk of serious infection

Side Efect

CNS: Dizziness, fever, headache
CV: Hypertension, hypotension
EENT: Nasopharyngitis, rhinitis, sinusitis
GI: Abdominal pain, diarrhea, diverticulitis, dyspepsia, nausea
GU: Acute pyelonephritis, UTI
MS: Back or limb pain
RESP: Bronchitis, COPD worsening, cough, dyspnea, pneumonia, upper respiratory tract infection, wheezing
SKIN: Cellulitis, flushing, pruritus, rash, urticaria
Other: Anaphylaxis, antibody formation, herpes simplex, herpes zoster infection, influenza, malignancies, varicella infection

Cautions

Screen patient for latent tuberculosis with a tuberculin skin test before starting abatacept. If test is positive, expect to provide A treatment, as ordered, before starting abatacept. Also screen patient for hepatitis B. If present, expect abatacept to be withdrawn because anti-rheumatic therapies such as abatacept may reactivate hepatitis B.

Review patient’s immunization record, and make sure all immunizations are current before therapy starts. Drug may blunt effectiveness of some vaccines and increase the risk of infection with live viruses.

Use cautiously in patients with a history of recurrent infections, underlying conditions that may predispose them to infection, or existing chronic, latent, or localized infection. They have an increased risk of infection with abatacept therapy.

Use cautiously in patients with COPD and monitor respiratory status closely because abatacept may worsen COPD and increase the risk of adverse respiratory reactions.

Tumor necrosis factor antagonists shouldn’t be given with abatacept because of an increased of serious infection.

Reconsititue each vial with 10 ml of sterile water for injection. Use only the siliconefree disposable syringe provided with each vial because a siliconized syringe may cause translucent particles to form in solution. After injecting sterile water into vial, gently swirl vial until contents are completely dissolved. To minimize foaming, don’t shake.Vent the vial with a needle to dissipate any foam that may be present.

Further dilute reconstituted solution with 0.9% sodium chloride injection to achieve a final solution of 100 ml. Slowly add solution into infusion bag or bottle using the same silicone-free disposable syringe provided with each vial. Mix gently. Do not shake the bag or bottle.

Give entire dose of fully diluted drug over 30 minutes using an infusion set and a sterile, nonpyrogenic, low protein-binding filter with a pore size of 0.2 µm.

Once fully diluted, solution may be kept for 24 hours at room temperature or refrigerated. If reconstituted solution isn’t used within 24 hours, discard.

After giving abatacept, monitor patient closely for evidence of hypersensitivity reaction such as rash, pruritus, urticaria, dyspnea, or wheezing. If present, stop drug immediately, notify prescriber, and provide emergency care, as ordered.

Monitor patient closely for evidence of infection or malignancy because abatacept inhibits T-cell activation, increasing the risk of these disorders.

PATIENT SAFTY

Instruct patient not to receive immunizations with live vaccines during abatacept therapy and for 3 months afterward.

Stress need to report any evidence of infection or hypersensitivity to prescriber.

Alert patient that abatacept may increase the risk of maligancy.

Warn patient to avoid crowds and people with infections.

Category

Chemical class: Fab fragment of chimeric 7E3 antibody
Therapeutic class: Platelet aggregation inhibitor

Pregnancy category: C

Indications

To prevent acute myocardial ischemic complications after percutaneous transluminal coronary angioplasty (PTCA) in patients at high risk for abrupt closure of treated coronary artery

IV

OR INJECTION
Adults. 250-mcg/kg bolus 10 to 60 min before PTCA. Maintenance: 0.125 mcg/kg/ min by continuous infusion for 12 hr. Maximum: 10 mcg/min. To treat unstable angina in patients who haven’t responded to conventional therapy and are scheduled for PTCA within 24 hr

IV

OR INJECTION
Adults. 250-mcg/kg by bolus; then 10 mcg/ min by continuous infusion over 18 to 24 hr, concluding 1 hr after PTCA. Route Onset Peak Duration I.V. Unknown Unknown 48 hr

Mechanism of Action

Binds to glycoprotein IIb/IIIa receptor sites on the surface of activated platelets. Circulating fibrinogen can bind to these receptor sites and link platelets together, abciximab 18 forming a clot that eventually blocks a coronary artery. By binding to receptor sites, abciximab prevents normal binding of fibrinogen and other factors and inhibits platelet aggregation.

Incompatibilities

Don’t mix abciximab with other . Give through separate I.V. line when possible.

Contraindications

Active internal bleeding, arteriovenous malformation or aneurysm, bleeding disorders, stroke in past 2 years or that caused significant neurologic deficit at any time, GI or GU bleeding in past 6 weeks, hypersensitivity to abciximab, intracranial neoplasm, I.V. dextran use before or during PTCA, oral anticoagulant therapy in past 7 days unless PT is less than 1.2 times control, severe uncontrolled hypertension, surgery in past 6 weeks, thrombocytopenia, vasculitis

Interactions

dipyridamole, heparin, NSAIDs, oral anticoagulants, thrombolytic , ticlopidine: Increased risk of bleeding

Side Efect

CNS: Confusion, dizziness, hyperesthesia
CV: Atrial fibrillation or flutter, bradycardia, embolism, hypotension, peripheral edema, pseudoaneurysm, supraventricular tachycardia, third-degree AV block, thrombophlebitis, weak pulse
GI: Dysphagia, hematemesis, nausea, vomiting
GU: Dysuria, hematuria, renal dysfunction, urinary frequency, urinary incontinence, urine retention
HEME: Anemia, bleeding, leukocytosis, thrombocytopenia
RESP: Bronchitis, bronchospasm, crackles, dyspnea, pleural effusion, pneumonia, pulmonary edema, pulmonary embolism, wheezing
SKIN: Pruritus, rash, urticaria
Other: Development of human antichimeric antibodies

Cautions

Know that abciximab may be used with heparin and aspirin therapy.

Inspect abciximab for particles; don’t use if opaque particles are present.

For continuous I.V. infusion, withdraw 4.5 ml from 2-mg/ml solution and inject prescribed amount into 250-ml bag of normal saline solution or D5W using an in-line sterile, nonpyrogenic, low–proteinbinding 0.2to 0.22-micron filter. Discard unused portion.

Give I.V. bolus with sterile, nonpyrogenic, low–protein-binding 0.2to 0.22-micron filter.

Avoid I.M. injections, venipunctures, and use of indwelling urinary catheters, NG tubes, and automatic blood pressure cuffs during therapy to prevent bleeding. If appropriate, insert an intermittent I.V. access device to obtain blood samples.

Watch for GI, GU, and retroperitoneal bleeding and bleeding at puncture sites.
WARNING If hemorrhage occurs, prepare to stop infusion immediately. Expect to treat severe thrombocytopenia with platelet transfusions if needed.

Monitor patient for hypersensitivity reactions, such as rash, pruritus, wheezing, and dysphagia from laryngeal edema. If such reactions occur, stop infusion and notify prescriber immediately. If anaphylaxis occurs, give epinephrine, antihistamines, and corticosteroids, as prescribed.

Obtain platelet count 2 to 4 hours after initial bolus and every 24 hours during therapy as ordered. Expect platelet function to return to normal within 48 hours after therapy ends.

Monitor vital signs and continuous ECG tracings during treatment.

PATIENT SAFTY

Teach about possible

Side Efect

, including bleeding and hypersensitivity reactions, which may cause rash, urticaria, and dyspnea.

Tell patient to prevent injury from falls by maintaining bed rest and from bleeding by keeping limb immobile while catheter sheath is in place.

Category

Chemical class: Synthetic endogenous amino acid homotaurine, gammaacamprosate calcium

Mechanism of Action

Chronic alcoholism may alter the balance between excitation and inhibition in neurons in the brain; acamprosate restores it. When the neurotransmitter gammaaminobutyric acid (GABA) binds to its receptors in the CNS, it opens the chloride ion channel and releases chloride (Cl-) into the cell (below left), thereby reducing neuronal excitability by inhibiting depolarization. By interacting with GABA receptor sites, acamprosate prevents GABA from binding (below right). When glutamate binds to its receptors, it closes the chloride ion channel, increasing neuronal excitability by promoting depolarization (below left). This imbalance fosters a craving for alcohol. By interacting with glutamate receptor sites, acamprosate prevents glutamate from binding (below right). aminobutyric acid (GABA) analogue
Therapeutic class: Antialcoholic

Pregnancy category: C

Indications

To maintain abstinence from alcohol for alcohol-dependent patients who are abstinent at the start of treatment
Adults. 666 mg t.i.d.
DOSAGE ADJUSTMENT For patients with moderate renal impairment (creatinine clearance of 30 to 50 ml/min), 333 mg t.i.d.

Contraindications

Hypersensitivity to acamprosate or its components, severe hepatic (Child-Pugh class C) or renal impairment

Interactions

antidepressants: Increased weight gain tetracyclines: Decreased absorption of tetracyclines

Side Efect

CNS: Abnormal thinking, amnesia, anxiety, asthenia, chills, depression, dizziness, headache, insomnia, paresthesia, somnolence, suicidal ideation, syncope, tremor
CV: Chest pain, hypertension, palpitations, peripheral edema, vasodilation
EENT: Abnormal vision, dry mouth, pharyngitis, rhinitis, taste perversion
GI: Abdominal pain, anorexia, constipation, diarrhea, flatulence, increased appetite, indigestion, nausea, vomiting
GU: Acute renal failure, decreased libido, impotence
HEME: Leukopenia, lymphocytosis, thrombocytopenia
MS: Arthralgia, back pain, myalgia
RESP: Bronchitis, cough, dyspnea
SKIN: Diaphoresis, pruritus, rash
Other: Flulike symptoms, infection, weight gain

Cautions

Acamprosate should start as soon as possible after patient has undergone alcohol withdrawal and achieved abstinence.

Continue to give acamprosate even during periods of alcohol relapse.

PATIENT SAFTY

Instruct patient to take acamprosate exactly as prescribed, even if a relapse occurs, and to seek help for a relapse.

Warn patient that acamprosate won’t reduce symptoms of alcohol withdrawal if relapse occurs followed by cessation.

Urge caregivers to monitor patient for evidence of depression (lack of appetite or interest in life, fatigue, excessive sleeping, difficulty concentrating) or suicidal tendencies because a small number of patients taking acamprosate have attempted suicide.

Advise patient to use caution when performing hazardous activities until adverse CNS effects of drug are known.

Tell female patient to notify prescriber if she is or intends to become pregnant while taking acamprosate; the drug may need to be stopped because fetal risks are unknown.

Category

Chemical class: Alpha-glucosidase inhibitor, oligosaccharide
Therapeutic class: Antidiabetic drug

Pregnancy category: B

Indications

To control blood glucose level in patients with type 2 (non–insulin-dependent) diabetes mellitus when the level can’t be controlled by diet alone
Adults.Initial: 25 mg t.i.d. with first bite of each meal. Maintenance: Increased to maximum at 4to 8-wk intervals p.r.n. Maximum: 50 mg t.i.d. for patients weighing 65 kg (143 lb) or less; 100 mg t.i.d. for patients weighing more than 65 kg.

Mechanism of Action

Inhibits action of alpha-amylase and alphaglucoside enzymes. Normally, alphaamylase hydrolyzes complex starches to oligosaccharides in the small intestine and alpha-glucoside hydrolyzes oligosaccharides, trisaccharides, and di-saccharides to glucose and other monosaccharides in the brush border of the small intestine. In diabetic patients, acarbose inhibits these actions and delays glucose absorption, reducing blood glucose level after meals.

Contraindications

Chronic intestinal disease, cirrhosis, colonic ulceration, conditions that may deteriorate because of increased gas formation in intestines, diabetic ketoacidosis, digestive or absorption disorders, history of bowel obstruction, hypersensitivity to acarbose, inflammatory bowel disease

Interactions

calcium channel blockers, digestive enzymes (such as pancreatin), diuretics, estrogen, intestinal adsorbents (such as activated charcoal), isoniazid, nicotinic acid, oral contraceptives, phenothiazines, phenytoin, sympathomimetics, thyroid hormones: Possibly decreased therapeutic effects of acarbose digoxin: Decreased serum level and therapeutic effects of digoxin insulin, sulfonylureas: Decreased insulin action, possibly increased risk of hypoglycemia

Side Efect

CV: Edema
GI: Abdominal distention and pain, diarrhea, flatulence, hepatitis, hepatotoxicity, ileus, jaundice
SKIN: Erythema, exanthema, rash, urticaria

Cautions

WARNING Be aware that acarbose isn’t recommended for patients with significant renal dysfunction and a serum creatinine level above 2 mg/dl.

If patient is receiving acarbose and a sulfonylurea or insulin to enhance glucose control, check blood glucose level often, as appropriate.

Store drug in sealed container in cool environment.

Expect to decrease dosage to control GI upset.

Monitor glycosylated hemoglobin level as ordered every 3 months for first year to evaluate glucose control and patient compliance.

Monitor hematocrit and serum AST level every 3 months during first year of therapy and periodically thereafter, as ordered, because acarbose may decrease hematocrit and increase serum AST level.

PATIENT SAFTY

Explain importance of self-monitoring glucose level during acarbose therapy.

Teach patient to recognize hypoglycemia and hyperglycemia.

Warn patient that noncompliance with treatment can increase risk of diabetic complications, including neuropathy, retinopathy, and renal insufficiency.

Explain that temporary insulin therapy may be needed if fever, trauma, infection, illness, surgery, or other stress alters blood glucose control.

Warn patient not to take other within 2 hours of acarbose unless specifically instructed by prescriber.

Tell him to consult prescriber before taking OTC during acarbose therapy.

Advise patient who also takes another antidiabetic to carry glucose with him at all times in case hypoglycemia occurs.

Category

Chemical class: Beta1-selective (cardioselective) adrenergic receptor blocker
Therapeutic class: Antihypertensive, class II antiarrhythmic

Pregnancy category: B

Indications

To treat hypertension
Adults.Initial: 400 mg daily or 200 mg b.i.d. Usual: 200 to 800 mg daily. Increased to 1,200 mg daily in divided doses b.i.d. for severe hypertension or hypertension that isn’t well controlled with usual dosage. To treat premature ventricular arrhythmias
Adults.Initial: 200 mg b.i.d. Usual: 600 to 1,200 mg daily.
DOSAGE ADJUSTMENT Maximum of 800 mg daily for elderly patients. Dosage reduced by 50% for patients with creatinine clearance less than 50 ml/min/1.73 m2. Dosage reduced by 75% for patients with creatinine clearance less than 25 ml/min/1.73 m2. Route Onset Peak Duration P.O. 1–1.5 hr 2–8 hr 24 hr or longer

Mechanism of Action

Inhibits stimulation of beta1receptors in the heart, decreasing cardiac excitability, heart rate, cardiac output, and myocardial oxygen demand. Acebutolol also decreases kidneys’ release of renin, which helps reduce blood pressure. Drug suppresses SA node automaticity and AV node conductivity, which suppresses atrial and ventricular ectopy. By decreasing myocardial oxygen demand, acebutolol decreases myocardial ischemia. At high doses, it inhibits stimulaacebutolol hydrochloride 22 tion of beta2receptors in the lungs and may cause bronchoconstriction.

Contraindications

Cardiogenic shock, heart failure unless from tachyarrhythmia, hypersensitivity to acebutolol, overt heart failure, secondand third-degree heart block, severe bradycardia

Interactions

alpha agonists, nasal decongestants: Increased risk of hypertension aluminum salts, barbiturates, calcium salts, cholestyramine, colestipol, indomethacin, NSAIDs, penicillins, rifampin, salicylates, sulfinpyrazone: Decreased antihypertensive effects anticholinergics, hydralazine, methyldopa, prazosin, reserpine: Increased risk of bradycardia and hypotension beta2agonists,
theophylline: Decreased bronchodilation epinephrine: Increased risk of blocked sympathomimetic effects ergot alkaloids: Increased risk of peripheral ischemia and gangrene flecainide: Possibly increased effects of both lidocaine: Possibly increased serum lidocaine level, causing toxicity oral contraceptives,
quinidine: Possibly increased serum acebutolol level sulfonylureas: Possibly decreased hypoglycemic effects verapamil: Increased cardiac effects, leading to bradycardia and hypotension

Side Efect

CNS: Abnormal dreams, anxiety, confusion, depression, dizziness, fatigue, fever, headache, insomnia
CV: Bradycardia, chest pain, edema, heart block, heart failure, hypotension
EENT: Abnormal vision, conjunctivitis, dry eyes, eye pain, pharyngitis, rhinitis
GI: Constipation, diarrhea, flatulence, hepatotoxicity, indigestion, nausea
GU: Dysuria, impotence, polyuria
MS: Arthralgia, myalgia
RESP: Bronchospasm, cough, dyspnea, wheezing
SKIN: Rash

Cautions

Before therapy begins, obtain baseline renal function tests, as ordered.

Check apical and radial pulses before giving acebutolol. Also, frequently monitor blood pressure and pulse rate, rhythm, and quality during treatment.

Give drug with food to prevent GI upset.

Acebutolol may elevate uric acid, potassium, triglyceride, lipoprotein, and antinuclear antibody levels; it also may interfere with accuracy of glucose tolerance tests.

Monitor diabetic patient’s blood glucose level to spot alterations.

Notify prescriber if you detect a heart rate below 50 beats/min or signs of heart failure, such as dyspnea, crackles, unexplained weight gain, and jugular vein distention.

Monitor patient for peripheral edema, and evaluate fluid intake and output.

PATIENT SAFTY

Tell patient that tablets may be crushed or swallowed whole.

Warn against stopping acebutolol abruptly because doing so could cause angina or dangerously high blood pressure.

Instruct patient to take a missed dose as soon as possible up to 6 hours before next scheduled dose but not to double the next dose.

Advise patient to consult prescriber before taking OTC that contain alpha agonists, such as nasal decongestants and cold preparations.

Instruct patient to report dizziness, confusion, and fever immediately.

Urge patient to maintain diet and lifestyle changes to help control blood pressure.

Category

Chemical class: Nonsalicylate, paraaminophenol derivative
Therapeutic class: Antipyretic, nonopioid analgesic

Pregnancy category: B

Indications

To relieve mild to moderate pain from headache, muscle ache, backache, minor arthritis, common cold, toothache, or menstrual cramps; to reduce fever CAPLETS, , CHEWABLE , ELIXIR, CAPLETS, GELCAPS, LIQUID, SOLUTION, SPRINKLES, SUSPENSION,
Adults.325 to 650 mg every 4 to 6 hr, or 1,000 mg t.i.d. or q.i.d., or 2 caplets every 8 hr. Maximum: 4,000 mg daily. Children over age 14. 650 mg every 4 hr. Maximum: 5 doses in 24 hr. Children ages 12 to 14. 640 mg every 4 hr. Maximum: 5 doses in 24 hr. Children age 11. 480 mg every 4 hr. Maximum: 5 doses in 24 hr. Children ages 9 to 10. 400 mg every 4 hr. Maximum: 5 doses in 24 hr. Children ages 6 to 8. 320 mg every 4 hr. Maximum: 5 doses in 24 hr. Children ages 4 to 5. 240 mg every 4 hr. Maximum: 5 doses in 24 hr. Children ages 2 to 3. 160 mg every 4 hr. Maximum: 5 doses in 24 hr. Children age 1. 120 mg every 4 hr. Maximum: 5 doses in 24 hr. Children ages 4 to 11 months. 80 mg every 4 hr. Maximum: 5 doses in 24 hr. Children ages 0 to 3 months. 40 mg every 4 hr. Maximum: 5 doses in 24 hr. SUPPOSITORIES Adults and adolescents. 650 mg every 4 to 6 hr. Maximum: 4,000 mg daily. Children ages 6 to 12. 325 mg every 4 to 6 hr. Maximum: 2,600 mg daily. Children ages 3 to 6. 120 to 125 mg every 4 to 6 hr. Maximum: 720 mg daily. Children ages 1 to 3. 80 mg every 4 hr. Children ages 3 months to 11 months. 80 mg every 6 hr.

Mechanism of Action

Inhibits the enzyme cyclooxygenase, blocking prostaglandin production and interfering with pain impulse generation in the peripheral nervous system. Acetaminophen also acts directly on temperature-regulating center in the hypothalamus by inhibiting synthesis of prostaglandin E2. Route Onset Peak Duration P.O., P.R. Varies 1–3 hr 3–4 hr

Contraindications

Hypersensitivity to acetaminophen or its components

Interactions

anticholinergics: Decreased onset of acetaminophen action barbiturates, carbamazepine, hydantoins, isoniazid, rifampin, sulfinpyrazone: Decreased therapeutic effects and increased hepatotoxic effects of acetaminophen lamotrigine, loop diuretics: Possibly decreased therapeutic effects of these oral contraceptives: Decreased effectiveness of acetaminophen probenecid: Possibly increased therapeutic effects of acetaminophen propranolol: Possibly increased action of acetaminophen zidovudine: Possibly decreased zidovudine effects
alcohol use: Increased risk of hepatotoxicity

Side Efect

GI: Abdominal pain, hepatotoxicity, nausea, vomiting
HEME: Hemolytic anemia (with long-term use), leukopenia, neutropenia, pancytopenia, thrombocytopenia
SKIN: Jaundice, rash, urticaria
Other: Angioedema, hypoglycemic coma

Cautions

Before and during long-term therapy, monitor liver function test results, including AST, ALT, bilirubin, and creatinine levels, as ordered.

Monitor renal function in patient on longterm therapy. Keep in mind that blood or albumin in urine may indicate nephritis; decreased urine output may indicate renal acetaminophen 24 failure; and dark brown urine may indicate presence of the metabolite phenacetin.

Expect to reduce dosage for patients with renal dysfunction.

Store suppositories under 80° F (26.6° C).
WARNING Be aware that Pediaphen is a concentrated form of acetaminophen containing 80 mg/0.8 ml (standard liquid forms contain 32 mg/ml). Make sure to use correct concentration and dosage of liquid acetaminophen because serious adverse reactions can result from confusing concentrated form with regular liquid form.

PATIENT SAFTY

Tell patient that tablets may be crushed or swallowed whole.

Instruct patient to read manufacturer’s label and follow dosage guidelines precisely. Explain that infants’ and children’s acetaminophen liquid aren’t equal in drug concentration and aren’t interchangeable.

Advise patient to use manufacturer’s dropper or dosage cup for measuring liquid acetaminophen.

Advise him to contact prescriber before taking other prescription or OTC products because they may contain acetaminophen.

Teach patient to recognize signs of hepatotoxicity, such as bleeding, easy bruising, and malaise, which commonly occurs with chronic overdose.

Category

Chemical class: Sulfonamide derivative
Therapeutic class: Anticonvulsant, antiglaucoma, diuretic

Pregnancy category: C

Indications

To treat chronic simple (open-angle) glaucoma S.R.,, I.V.OR
I.M.INJECTION
Adults. 250 to 1,000 mg daily (divided for doses exceeding 250 mg). As short-term therapy to treat secondary glaucoma and preoperatively to treat acute congestive (closed-angle) glaucoma S.R.,, I.V.OR
I.M.INJECTION
Adults.250 mg b.i.d. or every 4 hr; or 1 S.R. capsule (500 mg) b.i.d.; or 500 mg initially, followed by 125 to 250 mg every 4 to 6 hr for severe acute glaucoma. To initially lower intraocular pressure rapidly, 500 mg I.V.; may repeat in 2 to 4 hr in acute cases, depending on patient response. Oral therapy usually started after initial I.V. dose. S.R., Children.10 to 15 mg/kg daily in divided doses every 6 to 8 hr. I.V.OR
I.M.INJECTION Children. 5 to 10 mg/kg/dose every 6 hr. To induce diuresis in heart failure , I.V.OR
I.M.INJECTION
Adults.Initial: 250 to 375 mg or 5 mg/kg daily in morning. Maintenance: 250 to 375 mg or 5 mg/kg on alternate days or for 2 days followed by a drug-free day. To treat drug-induced edema , I.V.OR
I.M.INJECTION
Adults. 250 to 375 mg daily for 1 to 2 days. ,
I.V.INJECTION Children. 5 mg/kg/dose daily in morning. To treat seizures, including generalized tonic-clonic, absence, and mixed seizures, and myoclonic jerk patterns , I.V.OR
I.M.INJECTION Adults and children.8 to 30 mg/kg daily in divided doses. Optimal: 375 to 1,000 mg daily. When used with other anticonvulsants, 250 mg daily. To prevent or relieve symptoms of acute mountain sickness S.R.,
Adults.500 to 1,000 mg daily in divided doses, given 24 to 48 hr before ascent and continued for 48 hr or longer while at high altitude p.r.n. to control symptoms. Route Onset Peak Duration P.O. 1–1.5 hr 2–4 hr 8–12 hr P.O. (S.R.) 2 hr 8–12 hr 18–24 hr I.V. 2 min 15 min 4–5 hr

Mechanism of Action

Inhibits the enyzme carbonic anhydrase, which normally appears in the eyes’ ciliary processes, brain’s choroid plexes, and kidneys’ proximal tubule cells. In the eyes, enzyme inhibition decreases aqueous humor secretion, which lowers intraocular pressure. In the brain, inhibition may delay abnormal, intermittent, and excessive discharge from neurons that cause seizures. In the kidneys, it increases bicarbonate excretion, which carries out water, potassium, and sodium, thus inducing diuresis and metabolic acidosis. This acidosis counteracts respiratory alkalosis and reduces symptoms of mountain sickness, including headache, dizziness, nausea, and dyspnea.

Contraindications

Chronic noncongestive closed-angle glaucoma; cirrhosis; hyperchloremic acidosis; hypersensitivity to acetazolamide; hypokalemia; hyponatremia; severe pulmonary obstruction; severe renal, hepatic, or adrenocortical impairment

Interactions

amphetamines, methenamine, phenobarbital, procainamide,
quinidine: Decreased excretion and possibly toxicity of these corticosteroids: Increased risk of hypokalemia cyclosporine: Increased cyclosporine level, possibly nephrotoxicity or neurotoxicity diflunisal: Possibly significantly decreased intraocular pressure lithium: Increased excretion and decreased effectiveness of lithium primidone: Decreased serum and urine primidone levels salicylates: Increased risk of salicylate toxicity

Side Efect

CNS: Ataxia, confusion, depression, disorientation, dizziness, drowsiness, fatigue, fever, flaccid paralysis, headache, lassitude, malaise, nervousness, paresthesia, seizures, tremor, weakness
EENT: Altered taste, tinnitus, transient myopia
GI: Anorexia, constipation, diarrhea, hepatic dysfunction, melena, nausea, vomiting
GU: Crystalluria, decreased libido, glycosuria, hematuria, impotence, nephrotoxicity, phosphaturia, polyuria, renal calculi, renal colic, urinary frequency
HEME: Agranulocytosis, hemolytic anemia, leukopenia, pancytopenia, thrombocytopenia, thrombocytopenic purpura
SKIN: Photosensitivity, pruritus, rash, Stevens-Johnson syndrome, urticaria
Other: Acidosis, hyperuricemia, hypokalemia, weight loss

Cautions

Use acetazolamide cautiously in patients with calcium-based renal calculi, diabetes mellitus, gout, or respiratory impairment.

Know that acetazolamide may increase risk of hepatic encephalopathy in patients with hepatic cirrhosis.

To avoid painful I.M. injections (caused by alkaline solution), give acetazolamide by mouth or I.V. injection if possible.

Reconstitute each 500-mg vial with at least 5 ml sterile water for injection. Use within 24 hours because drug has no preservative.

Monitor blood tests during acetazolamide therapy to detect electrolyte imbalances.

Monitor fluid intake and output every 8 hours and body weight daily to detect excessive fluid and weight loss.

PATIENT SAFTY

Inform patient that acetazolamide tablets may be crushed and suspended in chocolate or another sweet syrup. Or, one tablet may be dissolved in 10 ml hot water and added to 10 ml honey or syrup.

Advise patient to avoid hazardous activities if dizziness or drowsiness occurs.

Instruct patient who takes high doses of salicylates to notify prescriber immediately about evidence of salicylate toxicity, such as anorexia, tachypnea, and lethargy.

If patient plans to mountain climb, urge her to descend mountain gradually and to seek immediate medical care if symptoms of mountain sickness occur.

Category

Chemical class: Sulfonylurea
Therapeutic class: Antidiabetic

Pregnancy category: C

Indications

To treat stable type 2 (non–insulindependent) diabetes mellitus
Adults.Initial: 250 to 1,500 mg daily. Dosages of 1,000 mg or more daily may be divided and given b.i.d. before morning and acetohexamide 26 evening meals.
DOSAGE ADJUSTMENT For patient being switched from another antidiabetic, acetohexamide dosage reduced to half the usual tolbutamide dosage or twice the usual chlorpropamide dosage. For patient being switched from insulin to acetohexamide monotherapy, dosages adjusted as follows: if insulin dosage is less than 20 units daily, acetohexamide starts at 250 mg daily and insulin is discontinued; if insulin dosage exceeds 20 units daily, acetohexamide starts at 250 mg daily and insulin is tapered by 25% to 30% before being reduced further according to patient response.

Mechanism of Action

Stimulates insulin release from active beta cells in the pancreas, resulting in decreased blood glucose level. Improves insulin binding to insulin receptors. Increases the number of insulin receptors (with long-term administration). May reduce basal hepatic glucose secretion.

Contraindications

Diabetes mellitus complicated by ketoacidosis or pregnancy, hypersensitivity to aceto-hexamide, renal failure, sole therapy for type 1 (insulin-dependent) diabetes mellitus

Interactions

activated charcoal: Possibly reduced absorption and effectiveness of acetohexamide androgens, anticoagulants, azole antifungals, chloramphenicol, clofibrate, fluconazole, gemfibrozil, H2-receptor antagonists, magnesium salts, MAO inhibitors, methyldopa, probenecid, salicylates, sulfinpyrazone, sulfonamides, tricyclic antidepressants, urinary acidifiers: Enhanced hypoglycemic effect of acetohexamide beta blockers, calcium channel blockers, cholestyramine, corticosteroids, diazoxide, estrogens, hydantoins, isoniazid, nicotinic acid, oral contraceptives, phenothiazines, rifampin, sympathomimetics, thiazide diuretics, thyroid , urinary alkalizers: Decreased hypoglycemic effect digitalis glycosides: Possibly increased serum digitalis level

Side Efect

CNS: Anxiety, chills, confusion, depression, dizziness, drowsiness, fatigue, headache, hyperesthesia, insomnia, malaise, nervousness, paresthesia, somnolence, syncope, tremor, vertigo, weakness
CV: Arrhythmias, edema, hypertension, vasculitis
EENT: Blurred vision, conjunctivitis, eye pain, pharyngitis, retinal hemorrhage, rhinitis, tinnitus
ENDO: Hypoglycemia
GI: Abdominal pain, anorexia, constipation, diarrhea, epigastric fullness, flatulence, heartburn, hepatitis, hepatotoxicity, indigestion, nausea, proctocolitis, vomiting
GU: Decreased libido, dysuria, polyuria
HEME: Agranulocytosis, aplastic anemia, eosinophilia, hemolytic anemia, leukopenia, pancytopenia, thrombocytopenia
MS: Abnormal gait, arthralgia, hypertonia, leg cramps
RESP: Dyspnea
SKIN: Diaphoresis, eczema, erythema multiforme, exfoliative dermatitis, flushing, jaundice, lichenoid reaction (skin thickening, accentuated lesions), maculopapular rash, photosensitivity, pruritus, rash, urticaria
Other: Disulfiram-like reaction (flushing, head throbbing, hypotension, nausea, tachycardia, vomiting), hyponatremia

Cautions

Use acetohexamide cautiously in elderly patients and in those with cardiac, hepatic, or renal disease or thyroid dysfunction. Drug’s duration of action is prolonged in patients with renal disease.

Give acetohexamide 30 minutes before meals, crushing tablets if desired. If GI upset occurs, give in divided doses, as prescribed.

Watch for evidence of hypoglycemia and hyperglycemia, especially after meals.

Check blood glucose level often, as ordered. Provide additional insulin if needed during stressful periods, as prescribed.

Monitor liver enzyme levels during therapy; acetohexamide may increase AST, ALT, and alkaline phosphatase levels.

Store acetohexamide in tightly sealed container in a cool environment.

PATIENT SAFTY

Stress need to adhere to prescribed drug regimen, diet, and exercise program.

Advise patient to take acetohexamide with food to avoid GI upset.

Teach patient how to self-monitor blood glucose level and check urine for glucose and ketones, as appropriate.

Teach patient to recognize and report signs of hypoglycemia and hyperglycemia.

Category

Chemical class: Synthetic hydroxylamine and ethylacetate derivative
Therapeutic class: Urease inhibitor

Pregnancy category: X

Indications

As an adjunct to antimicrobial therapy to treat chronic UTI caused by ureasplitting bacteria
Adults. Initial: 12 mg/kg daily in divided doses every 6 to 8 hr. Usual: 250 mg t.i.d. or q.i.d. for a total of 10 to 15 mg/kg daily. Maximum: 1,500 mg daily. Children. 10 mg/kg daily.
DOSAGE ADJUSTMENT Maximum dosage reduced to 1,000 mg daily or 500 mg every 12 hr for patients with serum creatinine level that exceeds 1.8 mg/dl.

Mechanism of Action

Inhibits urease, the enzyme that catalyzes urea’s hydrolysis to carbon dioxide and ammonia in urine infected with ureasplitting bacteria. This action reduces the urine ammonia level and pH, enhancing antimicrobial drug effectiveness.

Contraindications

Contributing disorder that’s treatable by surgery or appropriate antimicrobial therapy, hypersensitivity to acetohydroxamic acid, inadequate renal function (serum creatinine level above 2.5 mg/dl or creatinine clearance below 20 ml/min/1.73 m2), risk of pregnancy, UTI caused by non–ureaseproducing organisms, UTI that could be controlled by appropriate antimicrobial therapy

Interactions

iron: Decreased intestinal absorption of iron, decreased effects of iron and acetohydroxamic acid
alcohol use: Increased risk of severe rash 30 to 45 minutes after drinking alcohol

Side Efect

CNS: Anxiety, depression, fever, lack of coordination, malaise, headache, nervousness, slurred speech, tiredness, tremor
CV: Calf pain (deep vein blood clot), palpitations, sudden chest pain
EENT: Pharyngitis, sudden change in vision
GI: Anorexia, nausea, vomiting
HEME: Reticulocytosis, unusual bleeding
RESP: Dyspnea
SKIN: Ecchymosis, hair loss, nonpruritic macular rash

Cautions

Use acetohydroxamic acid cautiously in patients with severe chronic renal disease or anemia and those who’ve had phlebitis or thrombophlebitis.

Be aware that risk of adverse psychomotor effects increases if patient drinks alcohol or takes that affect alertness and reflexes, such as antihistamines, tranquilizers, sedatives, analgesics, and narcotics.

Administer tablets with food or liquid, crushing them if needed.
WARNING Acetohydroxamic acid chelates with dietary iron. If patient has iron deficiency anemia, expect to administer I.M. iron as needed during acetohydroxamic acid therapy.

Monitor follow-up laboratory tests to check renal and hepatic function and urine pH, as ordered.

PATIENT SAFTY

Instruct patient to take drug at same time each day, as prescribed.

Tell patient to take a missed dose up to 2 hours after scheduled time. If more than 2 hours have passed, he should wait for next scheduled dose and shouldn’t double that dose.

Warn patient not to take drug with alcohol or iron and to consult prescriber before taking it with any other drug. acetohydroxamic acid 28

Instruct patient to avoid hazardous activities during therapy.

Category

Chemical class: N-acetyl derivative of cysteine
Therapeutic class: Antidote (for acetaminophen overdose), mucolytic

Pregnancy category: B

Indications

To liquefy abnormal, viscid, or thickened mucus secretions in chronic pulmonary disorders (including emphysema, bronchitis, tuberculosis, bronchiectasis, and cystic fibrosis) and in pneumonia, pulmonary complications of thoracic or cardiovascular surgery, and tracheostomy care SOLUTION BY DIRECT INSTILLATION INTO TRACHEOSTOMY(MUCOMYST, MUCOSIL) Adults and children. 1 to 2 ml of 10% or 20% solution instilled every 1 to 4 hr, p.r.n. SOLUTION BY INHALATION Adults and children. 1 to 10 ml of 20% solution or 2 to 20 ml of 10% solution nebulized through face mask, mouthpiece, or tracheostomy every 2 to 6 hr. Usual: 3 to 5 ml of 20% solution or 6 to 10 ml of 10% solution t.i.d. or q.i.d. To treat acetaminophen overdose SOLUTION P.O.(MUCOMYST, MUCOSIL) Adults and children. Loading dose: 140 mg/ kg. Maintenance: 70 mg/kg 4 hr after loading dose and then every 4 hr to a total of 17 doses.
IV:(ACETADOTE) Adults and children weighing 40 kg (88 lb) or more. 150 mg/kg in 200 ml of diluent infused over 60 min, followed by 50 mg/kg in 500 ml of diluent infused over 4 hr, followed by 100 mg/kg in 1,000 ml of diluent infused over 16 hr. Adults and children weighing more than 20 kg (44 lb) but less than 40 kg. 150 mg/ kg in 100 ml of diluent infused over 60 min, followed by 50 mg/kg in 250 ml of diluent infused over 4 hr, followed by 100 mg/kg in 500 ml of diluent infused over 16 hr. Children weighing 20 kg or less. 150 mg/ kg in 3 ml/kg of diluent infused over 60 min, followed by 50 mg/kg in 7 ml/kg of diluent infused over 4 hr, followed by 100 mg/kg in 14 ml/kg of diluent infused over 16 hr.

Mechanism of Action

Decreases viscosity of pulmonary secretions by breaking disulfide links that bind glycoproteins in mucus. Reduces liver damage from acetaminophen overdose. Usually, acetaminophen’s toxic metabolites bind with glutathione in the liver, which detoxifies them. When acetaminophen overdose depletes glutathione stores, toxic metabolites bind with protein in liver cells, killing them. Acetylcysteine maintains or restores levels of glutathione or acts as its substitute, which reduces liver damage from acetaminophen overdose.

Incompatibilities

Don’t give acetylcysteine with nebulization equipment if drug can contact iron, copper, or rubber. Don’t give drug with amphotericin B, ampicillin sodium, chlortetracycline, chymotrypsin, erythromycin, hydrogen peroxide, iodized oil, oxytetracycline, tetracycline, or trypsin.

Contraindications

Hypersensitivity to acetylcysteine, no contraindications when used as antidote

Interactions

activated charcoal: Possibly adsorption and decreased effectiveness of oral acetylcysteine nitroglycerin: Increased effects of nitroglycerin and possibly significant hypotension and headache

Side Efect

CNS: Chills, dizziness, drowsiness, fever, headache
CV: Edema, hypertension, hypotension, tachycardia
EENT: Rhinorrhea, stomatitis, tooth damage
GI: Anorexia, constipation, hepatotoxicity, nausea, vomiting
RESP: Bronchospasm, chest tightness, cough, hemoptysis, respiratory distress, shortness of breath, stridor, wheezing
SKIN: Clammy skin, facial flushing, pruritus, rash, urticaria
Other: Anaphylaxis, angioedema

Cautions

Acetylcysteine should be used cautiously in patients with asthma or a history of bronchospasm because drug may adversely affect respiratory function.
WARNING To avoid fluid overload and possibly fatal hyponatremia or seizures, adjust total administered volume, as ordered, for patients weighing less than 40 kg (88 lb) and for those who need fluid restriction.

If needed, dilute 20% instillation or inhalation solution with normal saline solution or sterile water. The 10% solution may be used undiluted.

When treating acetaminophen overdose, dilute 20% oral solution with cola or other soft drink to a concentration of 5%, and use within 1 hour. Dilute parenteral solution with D5W or half-normal saline (0.45% sodium chloride) solution for injection following manufacturer guidelines because dilution is based on dosage. Acetadote may turn from colorless to slight pink or purple once the stopper is punctured, but color change has no effect on product quality.

Acetylcysteine is most effective if given within 24 hours of acetaminophen ingestion. For specific instructions, contact a regional poison center at 1-800-222-1222 or a special health professional assistance hotline at 1-800-525-6115.

If patient vomits loading dose or any maintenance dose within 1 hour of administration, repeat dose as prescribed.

Keep in mind that suicidal patient may not provide reliable information about vomiting. Watch such a patient to ensure that he ingests all of prescribed dosage.

During treatment for acetaminophen overdose, watch for signs of hepatotoxicity, such as prolonged bleeding time, altered coagulation, and easy bruising.

Be aware that acetylcysteine may have a disagreeable odor, which disappears as treatment progresses.

Because nebulization causes sticky residue on face and in mouth, have patient wash his face and rinse his mouth at the end of each treatment.

Be aware that an open vial of solution may turn light purple but that this doesn’t alter its effectiveness.

Refrigerate opened vials and discard after 96 hours.

Assess type, frequency, and characteristics of patient’s cough. Particularly note sputum. If cough doesn’t clear secretions, prepare to perform mechanical suctioning.

Monitor patient for tachycardia.

PATIENT SAFTY

Instruct patient to notify prescriber immediately about nausea, rash, or vomiting.

Warn patient about acetylcysteine’s unpleasant smell; reassure him that it subsides as treatment progresses.

To decrease mucus viscosity, urge patient to consume 2 to 3 L of fluid daily unless contraindicated by another condition.

Category

Chemical class: Synthetic retinoid
Therapeutic class: Antipsoriatic

Pregnancy category: X

Indications

To treat severe psoriasis
Adults. 25 to 50 mg once daily with a meal. Route Onset Peak Duration P.O. Unknown 2–5 hr Unknown

Mechanism of Action

Binds to several retinoid receptors to regulate gene transcription. Exactly how the action of this second-generation retinoid allows normal growth and development of skin is unknown.

Contraindications

Alcohol consumption; blood donation; breast-feeding; chronic hyperlipidemia; concurrent use of etretinate, methotrexate, or tetracycline; hypersensitivity to acitretin, other retinoids, or their components; pregnancy; severe hepatic or renal impairment

Interactions

methotrexate: Increased risk of hepatitis oral contraceptives containing only progestin: Possibly decreased effectiveness of oral contraceptive acitretin 30
phenytoin: Possibly decreased protein binding of phenytoin sulfonylureas: Possibly increased risk of hypoglycemia tetracyclines: Increased intracranial pressure vitamin A and other oral retinoids: Increased risk of hypervitaminosis A
alcohol use: Increased risk of adverse reactions and acitretin toxicity

Side Efect

CNS: Aggression, depression, fatigue, headache, hyperesthesia, hypotonia, insomnia, intracranial hypertension, paresthesia, peripheral neuropathy, rigors, somnolence, stroke, suicidal ideation, thirst
CV: Chest pain, decreased high-density lipoproteins, edema, elevated cholesterol or triglyceride levels, MI, thromboembolism
EENT: Abnormal or blurred vision, blepharitis, conjunctivitis, corneal epithelial abnormality, decreased night vision, deafness, dry eyes or mouth, earache, epistaxis, eye pain, gingival bleeding, gingivitis, increased saliva, photophobia, sinusitis, stomatitis, taste perversion, tinnitus, ulcerative stomatitits
ENDO: Hot flashes, hyperglycemia
GI: Anorexia, abdominal pain, diarrhea, elevated liver enzymes, hepatitis, hepatotoxicity, nausea, pancreatitis
GU: Vulvovaginitis
HEME: Hemorrhage, increased bleeding time
MS: Arthralgia, arthrosis, back pain, hyperostosis, myalgia, myopathy
SKIN: Abnormal skin or hair texture, alopecia, bullous eruption, cold or clammy skin, dermatitis, diaphoresis, dry or peeling skin, erythematous rash, flushing, fragility or thinning of skin, photosensitivity, pruritus, purpura, pyogenic granuloma, rash, scaling, seborrhea, skin fissure or ulceration
Other: Hypervitaminosis A, increased appetite

Cautions

WARNING Don’t give acitretin to a pregnant woman, a woman contemplating pregnancy, or a woman who may not use reliable contraception during drug therapy and for at least 3 years afterward because acitretin causes major fetal abnormalities.

Make sure patient has had two negative urine or serum pregnancy tests with a sensitivity of at least 25 mIU/ml before receiving acitretin. First test should be obtained when decision is made to use acitretin and second test during first 5 days of the menstrual period just before acitretin therapy starts. For patients with amenorrhea, second test should be done at least 11 days after the last act of unprotected sexual intercourse (which means without using two effective forms of contraception simultaneously).

Check to make sure female patient of childbearing age has signed the patient agreement and informed consent form before starting acitretin therapy.

Obtain a lipid profile, as ordered, before acitretin therapy starts and every 1 to 2 weeks for up to 8 weeks or until lipid effects are known. In high-risk patients, such as those with diabetes, obesity, or a history of alcohol abuse and those taking acitretin long-term, check lipid profile periodically throughout therapy.

Monitor liver function test results, as ordered. If hepatotoxicity is suspected, expect to stop drug and investigate cause.

If patient takes acitretin long-term or she develops a skeletal disorder, prepare her for periodic bone radiography because ossification abnormalities can occur, especially of the vertebral column, knees, and ankles.

Monitor patient’s eyes for abnormalities throughout therapy. Expect patient to stop drug and have an ophthalmologic examination if eye abnormalities occur.

Monitor patient for evidence of increased intracranial pressure, such as papilledema, headache, nausea, vomiting, and visual disturbances. If papilledema occurs, stop drug therapy immediately and obtain a neurologic evaluation, as ordered. Patient should never receive a tetracycline while taking acitretin because combined use can increase intracranial pressure.

Assess patient for suidical ideation because depression and other psychiatric symptoms, including thoughts of self-harm, may occur with acitretin use. Expect drug to be discontinued if psychiatric symptoms develop.

Significantly lower doses of phototherapy are needed during acitretin therapy because drug increases the risk of erythema.

PATIENT SAFTY

WARNING Warn women of childbearing age that acitretin causes major fetal abnormalities.

Inform woman of childbearing age that she must have a pregnancy test before acitretin therapy starts, every month during acitretin therapy, and every 3 months for 3 years after therapy stops.

Stress to woman of childbearing age that she must use two effective forms of contraception simultaneously unless she has chosen absolute abstinence or has had a hysterectomy. This must begin at least 1 month before acitretin therapy starts and continue throughout therapy and for at least 3 years after therapy ends.

Caution women taking oral contraceptives that some prescribed and OTC , including herbal supplements such as St. John’s wort, may interfere with oral contraceptives. Urge her to tell prescriber about all she takes.

Caution patient not to consume alcohol or products that contain alcohol during acitretin therapy and for 2 months after therapy ends.

Warn patient, male or female of any age, not to donate blood during acitretin therapy and for at least 3 years after it ends.

Review acitretin medication guide with patient, and answer the patient’s questions.

Inform patient that psoriasis may worsen during initial treatment and that full effects of drug may not be seen for up to 3 months.

Caution patient to avoid hazardous activities until drug’s CNS and ophthalmic effects are known.

Inform patient that tolerance to contact lenses may decrease during acitretin therapy and for a period of time after treatment ends.

Advise patient not to take more than the minimum recommended daily allowance of vitamin A during acitretin therapy because of the risk of vitamin A toxicity.

Caution patient not to use sun lamps and to avoid excessive exposure to sunlight because the effects of UV light are enhanced by retinoids such as acitretin.

Category

Chemical class: Recombinant human IgG1 monoclonal antibody
Therapeutic class: Disease-modifying antirheumatic

Pregnancy category: B

Indications

To reduce signs and symptoms, induce major clinical response, inhibit progression of structural damage, and improve physical function in patients with moderately to severely active rheumatoid arthritis; to reduce signs and symptoms, inhibit progression of structural damage, and improve physical function in patients with psoriatic arthritis; to reduce signs and symptoms in patients with active ankylosing spondylitis SUBCUTANEOUS INJECTION
Adults. 40 mg every other wk.
DOSAGE ADJUSTMENT Dosage may be adjusted to 40 mg every wk, as needed and prescribed, for patients not taking methotrexate. To reduce signs and symptoms and induce and maintain clinical remission in patients with moderately to severely active Crohn’s disease who have had an inadequate response to conventional therapy or who have stopped responding to or have become intolerant of infliximab SUBCUTANEOUS INJECTION
Adults.Initial: 40 mg q.i.d. for 1 day or 40 mg b.i.d. for 2 consecutive days, followed by 80 mg 2 wk later. Maintenance: 40 mg every other wk starting at week 4. To reduce signs and symptoms of moderately to severely active polyarticular juvenile idiopathic arthritis SUBCUTANEOUS INJECTION Children age 4 and over who weigh 30 kg (66 lb) or more.40 mg every other wk. Children age 4 and over who weigh less than 30 kg but at least 15 kg (33 lb). 20 mg every other wk. To treat moderate to severe chronic plaque psoriasis in patients who are adalimumab 32 candidates for systemic therapy or phototherapy, and when other systemic therapies are less appropriate SUBCUTANEOUS INJECTION
Adults. Initial: 80 mg followed 1 wk later with 40 mg. Maintenance: 40 mg every other wk.

Mechanism of Action

Binds to tumor necrosis factor (TNF) to block interaction with p55 and p75 cellsurface TNF receptors, and lyses surface TNF-expressing cells in the presence of complement. TNF may be a major component of rheumatoid arthritis inflammation and joint destruction. Reduced TNF level in synovial fluid improves signs and symptoms and prevents further structural damage in rheumatoid arthritis.

Contraindications

Active infection, breast-feeding, hypersensitivity to adalimumab or its components

Interactions

anakinra: Possibly increased risk of serious infection and neutropenia live vaccines: Increased risk of adverse vaccine effects

Side Efect

CNS: Confusion, fever, headache, hypertensive encephalopathy, multiple sclerosis, paresthesia, subdural hematoma, syncope, tremor
CV: Arrhythmias, atrial fibrillation, cardiac arrest, chest pain, coronary artery disease, congestive heart failure, hypercholesterolemia, hyperlipidemia, hypertension, MI, palpitations, pericardial effusion, pericarditis, peripheral edema, tachycardia
EENT: Cataracts, sinusitis
ENDO: Ketosis, parathyroid disorder
GI: Abdominal pain, cholecystitis, cholelithiasis, diverticulitis, elevated alkaline phosphatase level, elevated liver enzyme levels, esophagitis, gastroenteritis, hemorrhage, hepatic necrosis, nausea, vomiting
GU: Hematuria, paraproteinemia, pyelonephritis, UTI
HEME: Agranulocytosis, aplastic anemia, granulocytopenia, leukopenia, lymphocytosis, pancytopenia, polycythemia, thrombocytopenia
MS: Arthritis (including pyogenic or septic arthritis); back, extremity, pelvic, or thorax pain; bone disorder, fracture, or necrosis; muscle spasms; myasthenia; prosthetic infections; synovitis
RESP: Asthma, bronchitis, bronchospasm, decreased pulmonary function, dyspnea, pleural effusion, pneumonia, pulmonary tuberculosis, upper respiratory tract infection
SKIN: Cellulitis, erysipelas, erythema multiforme, herpes zoster, new or worsening psoriasis, rash, urticaria
Other: Anaphylaxis; antibody formation against adalimumab; dehydration; flare-up of disease process; flulike symptoms; healing abnormalities; injection site erythema, hemorrhage, itching, pain, or swelling; invasive fungal infection; lupus-like symptoms; lymphomas; malignancies; opportunistic infection; postsurgical infection; sepsis; tuberculosis (miliary, lymphatic, or peritoneal)

Cautions

Use adalimumab cautiously in patients with recurrent infection or increased risk of infection, patients who live in regions where tuberculosis and mycoses are endemic, and patients with a history of CNS demyelinating disorders because they occur, rarely, during adalimumab therapy.
WARNING If patient has evidence of an active infection when drug is prescribed, therapy shouldn’t start until infection has been treated. Monitor all patients for infection during therapy, especially those receiving immunosuppressants. If a serious infection develops, expect prescriber to stop drug.

Make sure patient has a tuberculin skin test before therapy starts. If skin test is positive, treatment of latent tuberculosis will start before adalimumab, as prescribed.

Be aware that the needle cover of the syringe contains dry rubber. Don’t handle if you’re allergic to latex.

To activate the protection device on needles of prefilled syringes delivered to institutions, hold the syringe in one hand and, with the other hand, slide outer protective shield over exposed needle until it locks into place.
WARNING Stop adalimumab immediately and tell prescriber if patient has an allergic reaction. Expect to provide supportive care.

Watch closely for evidence of congestive heart failure (sudden, unexplained weight gain; dyspnea; crackles; anxiety), and notify prescriber if they occur.

Monitor patient’s CBC, as ordered, because adalimumab may have adverse hematologic effects. Notify prescriber about persistent fever, bruising, bleeding, or pallor.

Be aware that adalimumab belongs to a group of called tumor necrosis factor (TNF) blockers. Although rare, malignancies, especially lymphomas and leukemias, have occurred in patients receiving TNF blockers, including children. Patients with rheumatoid arthritis, especially those with very active disease, are at greatest risk. Monitor patients closely.

PATIENT SAFTY

vInform patient that the first injection of adalimumab must take place with a health care professional present.

Teach patient or caregiver how to give adalimumab as a subcutaneous injection at home, if applicable. Emphasize importance of injecting the full amount in the syringe (0.8 ml) to obtain the correct dose of 40 mg.

If patient is allergic to latex, explain that the needle cover contains rubber.

Caution patient against reusing needles and syringes. Provide patient or caregiver with a puncture resistant container for disposal of needles and syringes at home.

Instruct patient or caregiver to rotate injection sites and to avoid injecting in any area that’s tender, bruised, red, or hard.

Inform patient that prefilled syringes must be refrigerated (not frozen), protected from light, and stored in the original container.

Urge patient to check expiration dates and not to use outdated drug.

Review signs and symptoms of an allergic reaction (rash, swollen face, difficulty breathing), and tell patient to seek emergency care immediately if these occur.

Inform patient that injection site reactions (such as redness, rash, swelling, itching, and bruising) may occur but are usually mild and transient. Instruct him to apply a towel soaked with cold water on the injection site if it hurts or remains swollen. If reaction does not disappear or seems to worsen, tell patient to call prescriber immediately.

Inform patient that tuberculosis may occur during adalimumab therapy. Instruct him to report persistent cough, wasting or weight loss, and low-grade fever to prescriber.

Teach patient to recognize evidence of infection and bleeding disorders and to tell prescriber if they occur; drug may need to be stopped. Advise patient to avoid people with infections and to have all prescribed laboratory tests.

Inform patient that the risk of certain kinds of cancer, especially lymphomas, is higher in patients taking adalimumab but still rare. Emphasize the importance of follow-up visits and reporting an unusual or sudden onset of signs or symptoms.

Caution patient against receiving livevirus vaccines while taking adalimumab because doing so may adversely effect the immune system.

Inform patient that blood samples may be needed periodically, but especially around week 24 of therapy, to check for autoantibody development. Explain that adalimumab therapy will need to be stopped if they’re detected.

Instruct patient to report lupus-like signs and symptoms that, although rare, may occur during therapy, such as chest pain that doesn’t go away, shortness of breath, joint pain, or a rash on cheeks or arms that’s sensitive to the sun. Explain that drug may be stopped if these occur.

Advise patient to inform all health care providers about adalimumab use and to inform prescriber about any OTC medications being taken, including herbal remedies and vitamin and mineral supplements.

Category

Chemical class: Monophosphorylated adenine riboside adenosine 34
Therapeutic class: Antiarrhythmic

Pregnancy category: C

Indications

To convert paroxysmal supraventricular tachycardia (PSVT) to normal sinus rhythm
I.V.INJECTION Adults and children weighing 50 kg (110 lb) or more. Initial: 6 mg by rapid peripheral I.V. bolus over 1 to 2 sec. If PSVT continues after 1 to 2 min, 12 mg given as rapid bolus and repeated in 1 to 2 min if needed. Don’t give single doses of more than 12 mg. Children weighing less than 50 kg. Initial: 0.05 to 0.1 mg/kg as rapid central or peripheral I.V. bolus followed by saline flush. If PSVT continues after 1 to 2 min, additional bolus injections are given, incrementally increasing dose by 0.05 to 0.1 mg/ kg. Follow each bolus with saline flush. Injections continue until PSVT converts to normal sinus rhythm or until patient reaches maximum single dose of 0.3 mg/kg. Route Onset Peak Duration I.V. Immediate Immediate Unknown

Mechanism of Action

Slows conduction time through the AV node and can interrupt AV node reentry pathways to restore normal sinus rhythm.

Incompatibilities

Don’t mix adenosine with other .

Contraindications

Atrial fibrillation or flutter; hypersensitivity to adenosine; secondor third-degree heart block or sick sinus syndrome, except in patients with a functioning artificial pacemaker; ventricular tachycardia

Interactions

carbamazepine: Increased heart block digoxin, verapamil: Possibly increased depressant effect on SA or AV node dipyridamole: Increased adenosine effects methylxanthines, such as
theophylline: Antagonized adenosine effects caffeine: Antagonized adenosine effects

Side Efect

CNS: Apprehension, dizziness, headache, heaviness in arms, light-headedness, nervousness, paresthesia, seizures
CV: Atrial fibrillation, bradycardia, chest pain or pressure, heart block, hypertension, hypotension, MI, palpitations, prolonged asystole, sinus exit block or pause, torsades de pointes, transient hypertension, ventricular fibrillation, ventricular tachycardia
EENT: Blurred vision, metallic taste, throat tightness
GI: Nausea, vomiting
MS: Jaw, neck, and back pain
RESP: Bronchoconstriction, bronchospasm, dyspnea, hyperventilation, respiratory arrest
SKIN: Diaphoresis, facial flushing
Other: Injection site reaction

Cautions

Before use, inspect adenosine for crystals. If solution isn’t clear, don’t give it.

Give adenosine by rapid I.V. bolus over 1 to 2 seconds. Slower delivery can cause systemic vasodilation and reflex tachycardia.

Expect prescriber to inject adenosine directly into a vein to make sure drug reaches systemic circulation. If given into an I.V. line, give drug as close to insertion site as possible and follow with rapid saline flush.
WARNING Don’t give single doses of more than 12 mg.

Monitor heart rate and rhythm, blood pressure, and respiratory status often during adenosine therapy.

Be aware that at the time of conversion to normal sinus rhythm, arrhythmias (such as PVCs, premature atrial contractions, sinus bradycardia, sinus tachycardia, and AV block) may occur for a few seconds, but they don’t usually require intervention.
WARNING Stop drug use and notify prescriber immediately if severe respiratory difficulties develop.

Store adenosine at room temperature. Discard unused portion.

PATIENT SAFTY

Instruct patient to report chest pain, palpitations, difficulty breathing, or severe headache during adenosine therapy.

Warn patient that mild, temporary reactions may occur, such as flushing, nausea, and dizziness. alatrofloxacin mesylate Trovan I.V.

Category

Chemical class: Fluoroquinolone
Therapeutic class: Antibacterial

Pregnancy category: C

Indications

To treat life-threatening nosocomial pneumonia ,

IV

Adults.300 mg I.V. every 24 hr followed by 200 mg P.O. every 24 hr when patient is stabilized for total of 10 to 14 days. To treat life-threatening communityacquired pneumonia ,
IV:
Adults. 200 mg I.V. every 24 hr followed by 200 mg P.O. every 24 hr when patient is stabilized for total of 7 to 14 days; or 200 mg P.O. every 24 hr for total of 7 to 14 days. To treat complicated, life-threatening intra-abdominal infections, including postsurgical, gynecologic, and pelvic infections ,
IV:
Adults. 300 mg I.V. every 24 hr followed by 200 mg P.O. every 24 hr when patient is stabilized for total of 7 to 14 days. To treat complicated, life-threatening or limb-threatening skin and soft-tissue infections, including diabetic foot infections ,
IV:
Adults.200 mg P.O. every 24 hr—or 200 mg I.V. every 24 hr followed by 200 mg P.O. every 24 hr when patient is stabilized—for total of 10 to 14 days.
DOSAGE ADJUSTMENT For patients with mild to moderate cirrhosis, 300-mg I.V. dosage reduced to 200 mg and 200-mg I.V. and P.O. dosage reduced to 100 mg.

Mechanism of Action

Interferes with DNA gyrase, the enzyme needed for DNA replication in aerobic and anaerobic bacteria. May be active against pathogens resistant to such antibiotics as penicillins, cephalosporins, aminoglycosides, macrolides, and tetracyclines.

Incompatibilities

Don’t mix alatrofloxacin with or infuse it simultaneously through same I.V. line as other . Don’t dilute it with normal saline solution or lactated Ringer’s solution.

Contraindications

Hypersensitivity to alatrofloxacin, quinolone antimicrobials, trovafloxacin, or their components

Interactions

antacids that contain aluminum, citric acid, magnesium, or sodium citrate; iron; morphine sulfate; sucralfate: Reduced absorption of trovafloxacin

Side Efect

CNS: Dizziness, headache, light-headedness, seizures
CV: Hypotension
EENT: Hoarseness, throat tightness
GI: Abdominal pain, acute hepatic failure (anorexia, dark urine, dysphagia, fatigue, jaundice, pale stool, and vomiting)
GU: Vaginitis
RESP: Dyspnea
SKIN: Photosensitivity, rash, urticaria or other skin reactions
Other: Angioedema

Cautions

Infuse alatrofloxacin over 60 minutes; rapid or bolus I.V. delivery may cause hypotension.

Periodically assess patient’s liver function test results. Results may be elevated for up to 21 days after alatrofloxacin use.
WARNING Be aware that alatrofloxacin may cause severe liver damage, requiring liver transplantation or leading to death. Expect therapy to last no longer than 2 weeks to reduce risk of liver damage. Alatrofloxacin is reserved for hospitalized patients with lifeor limb-threatening infections.

PATIENT SAFTY

Instruct patient to report rash; urticaria; trouble swallowing; swelling of the lips, face, or tongue; hoarseness; or throat tightness.

Category

Chemical class: Selective beta2-adrenergic agonist, sympathomimetic
Therapeutic class: Bronchodilator

Pregnancy category: C

Indications

To prevent exercise-induced asthma INHALATION AEROSOL Adults and children over age 4. 2 inhalations 15 to 30 min before exercise. To treat bronchospasm in patients with reversible obstructive airway disease or acute bronchospastic attack Adults and children over age 12. Initial: 4 or 8 mg every 12 hr. Maximum: 32 mg daily in divided doses every 12 hr. Children ages 6 to 12. Initial: 4 mg every 12 hr. Maximum: 24 mg daily in divided doses every 12 hr. REPETABS Adults and children over age 12. Initial: 4 to 8 mg every 12 hr. Maximum: 32 mg daily in divided doses every 12 hr. Children ages 6 to 11. Initial: 4 mg every 12 hr. Maximum: 24 mg daily in divided doses every 12 hr. SYRUP Adults and children over age 14. Initial: 2 to 4 mg (1 to 2 tsp) t.i.d. or q.i.d. Maximum: 32 mg daily in divided doses. Children ages 6 to 14. Initial: 2 mg (1 tsp) t.i.d. or q.i.d. Maximum: 24 mg daily in divided doses. Children ages 2 to 6. Initial: 0.1 mg/kg t.i.d. (not to exceed 2 mg t.i.d.), increased to 0.2 mg/kg t.i.d. (not to exceed 4 mg t.i.d.). Adults and children over age 12. Initial: 2 or 4 mg t.i.d. or q.i.d. Maximum: 32 mg daily in divided doses. Children ages 6 to 12. Initial: 2 mg t.i.d. or q.i.d. Maximum: 24 mg daily in divided doses.
DOSAGE ADJUSTMENT For elderly patients, initial dosage reduced to 2 mg (1 tsp) of syrup t.i.d. or q.i.d. or 2 mg of tablets t.i.d. or q.i.d. (up to 32 mg daily). INHALATION AEROSOL Adults and children age 4 and over. 1 inhalation every 4 hr to 2 inhalations every 4 to 6 hr. INHALATION (ROTOCAPS) Adults and children age 4 and over. 200 mcg inhaled every 4 to 6 hr using inhalation device. Maximum: 400 mcg every 4 to 6 hr. INHALATION SOLUTION Adults and children age 12 and over. 2.5 mg t.i.d. or q.i.d. by nebulization over 5 to 15 min. Children ages 2 to 12. Initial: 0.1 to 0.15 mg/kg t.i.d. or q.i.d. Maximum: 2.5 mg t.i.d. or q.i.d. Route Onset Peak Duration P.O. ( tab) 30 min 2–3 hr 12 hr P.O. (syrup) Rapid 2 hr Unknown P.O. (tab) 30 min 2–3 hr 4–8 hr Inhalation 5–15 50–55 3–6 hr (aerosol) min min Inhalation 5–15 0.5–3 2–6 hr (rotocap) min hr Inhalation 5–15 1–2 hr 3–6 hr (solution) min

Contraindications

Hypersensitivity to albuterol or its components

Interactions

beta blockers: Inhibited effects of albuterol bronchodilators (sympathomimetics), such as
theophylline: Possibly adverse CV effects digoxin: Decreased serum digoxin level MAO inhibitors, tricyclic antidepressants: Increased vascular effects of albuterol methyldopa: Increased vasopressor effect of methyldopa potassium-lowering : Possibly hypokalemia potassium-wasting diuretics: Possibly increased hypokalemia

Side Efect

CNS: Anxiety, dizziness, drowsiness, headache, hyperkinesia, insomnia, irritability, nervousness, tremor, vertigo, weakness
CV: Angina; arrhythmias, including atrial fibrillation, extrasystoles, supraventricular tachycardia, and tachycardia; chest pain; hypertension; hypotension; palpitations
EENT: Altered taste, dry mouth and throat, ear pain, glossitis, hoarseness, oropharyngeal edema, pharyngitis, rhinitis, taste perversion
ENDO: Hyperglycemia
GI: Anorexia, diarrhea, dysphagia, heartburn, nausea, vomiting
GU: UTI
MS: Muscle cramps
RESP: Bronchospasm, cough, dyspnea, paradoxical bronchospasm, pulmonary edema
SKIN: Diaphoresis, flushing, pallor, pruritus, rash, urticaria
Other: Angioedema, hypokalemia, infection, metabolic acidosis

Cautions

Administer pressurized inhalations of albuterol during second half of inspiration, when airways are open wider and aerosol distribution is more effective.
WARNING Use cautiously in patients with cardiac disorders, diabetes mellitus, digitalis intoxication, hypertension, hyperthyroidism, or history of seizures. Albuterol can worsen these conditions.

Monitor serum potassium level because albuterol may cause transient hypokalemia.

Be aware that drug tolerance can develop with prolonged use.

PATIENT SAFTY

Teach patient to use inhaler. Tell him to shake canister before use and to check that a new canister is working by spraying it the appropriate number of times (once to four times based on manufacturer instructions) into the air while looking for a fine mist.

Instruct patient to wash mouthpiece with water once a week and let it air-dry.

Advise patient to wait at least 1 minute between inhalations.

Tell patient to check with his prescriber before using other inhaled .

Warn patient not to exceed prescribed dose or frequency. If doses become less effective, tell patient to contact his prescriber.

Tell patient to immediately report signs and symptoms of allergic reaction, such as difficulty swallowing, itching, and rash.

Category

Chemical class: Recombinant leukocyte function-associated antigen-3 immunoglobulin GI fusion protein
Therapeutic class: Immunosuppresant

Pregnancy category: B

alefacept 38 cAMP ATP Adenylate cyclase Albuterol Beta2 receptor Bronchial cell membrane Albuterol attaches to beta2receptors on bronchial cell membranes, which stimulates the intracellular enzyme adenylate cyclase to convert adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP). This reaction decreases intracellular calcium levels. It also increases intracellular levels of cAMP, as shown. Together, these effects relax bronchial smooth-muscle cells and inhibit histamine release.

Mechanism of Action

Indications

To treat moderate to severe chronic plaque psoriasis in patients who are candidates for systemic therapy or phototherapy I.V. INJECTION
Adults. Initial: 7.5 mg every wk for 12 wk. After at least 12 wk in which drug isn’t given, a second 12-wk course may be given, if needed and if patient’s CD4 and T-lymphocyte counts are within normal ranges.
I.M.INJECTION
Adults. 15 mg every week for 12 wk. After at least 12 wk in which drug isn’t given, a second 12-wk course may be given, if needed and if patient’s CD4 and T-lymphocyte counts are within normal ranges.

Mechanism of Action

Interferes with T-lymphocyte activation by binding to lymphocyte antigen and CD2, inhibiting LFA-3/CD2 interaction, and reducing the subsets of CD2+ T lymphocytes. This interference helps prevent plaque formation in chronic plaque psoriasis.

Incompatibilities

Don’t add other to solutions containing alefacept.

Contraindications

Breast-feeding, hypersensitivity to alefacept or its components

Side Efect

CNS: Chills, dizziness, headache
CV: Coronary artery disease, MI
EENT: Pharyngitis
GI: Nausea
HEME: Lymphopenia
MS: Myalgia
RESP: Increased cough
SKIN: Pruritus, urticaria
Other: Angioedema, injection site pain or inflammation, infection, malignancies

Cautions

Use alefacept cautiously in patients at high risk for malignancy because the drug increases risk of malignancy development. Know that drug isn’t recommended for use in patients with a history of a systemic malignancy.

Also use alefacept cautiously in patients with chronic infections or history of recurrent infection. Drug may increase risk of infection because of its immunosuppressive action.

Obtain a CD4+ and T-lymphocyte count before starting alefacept therapy, as ordered. If counts are below normal, be aware that therapy shouldn’t be started. After therapy starts, monitor patient’s CD4+ and T-lymphocyte counts weekly throughout therapy. If levels drop below 250 cells/microliter, notify prescriber because drug will need to be withheld. If counts remain below 250 cells/microliter for 1 month, expect that drug will be discontinued.

Reconstitute drug with 0.6 ml using only the supplied diluent (sterile water for injection) before administration. With the needle pointed at sidewall of vial, slowly inject diluent into vial of alefacept. Be aware that some foaming will occur. To prevent excessive foaming, don’t shake or vigorously agitate vial. Instead, gently swirl vial during dissolution, which usually takes less than 2 minutes.

Administer drug as soon as possible after reconstitution. Discard solution if not used within 4 hours.

Don’t filter reconstituted solution during preparation or administration.

For I.M. administration, inject the full 0.5 ml of solution. Use a different injection site for each subsequent injection, injecting at least 1 inch away from previous sites. Never inject the drug into tender, bruised, red, or hard areas.

For I.V. administration, prepare two syringes with 3 ml normal saline solution for preadministration and postadministration flush. Then prime the winged infusion set with 3 ml normal saline solution and insert into vein. Attach filled syringe to infusion set, and administer solution over no more than 5 seconds. Finish by flushing set with 3 ml of normal saline solution.

Be aware that drug shouldn’t be started in a patient with a concurrent serious infection. Monitor patient closely during and after therapy for signs and symptoms of infection. If these occur, report them to the prescriber immediately and begin treatment, as prescribed, to reduce risk of serious infection. If infection becomes serious, expect drug to be discontinued.

Monitor patient for allergic reactions. If these occur, discontinue drug and notify prescriber immediately.

PATIENT SAFTY

Advise patient that weekly blood tests will be required to monitor his WBC count during alefacept therapy.

Teach patient signs and symptoms of infection and common
WARNING signs of malignancy. Emphasize importance of complying with follow-up visits and promptly reporting any unusual or sudden signs or symptoms suggesting malignancy or infection.

Instruct female patient to notify prescriber if she becomes pregnant while taking alefacept or within 8 weeks after stopping it.

Category

Chemical class: Aminobisphosphonate
Therapeutic class: Bone resorption inhibitor

Pregnancy category: C

Indications

To prevent postmenopausal osteoporosis
Adults.5 mg daily or 35 mg once/wk in the morning with a full glass of water at least 30 min before first food, drink, or drug. To treat postmenopausal osteoporosis
Adults. 10 mg daily or 70 mg once/wk in the morning with a full glass of water at least 30 min before first food, drink, or drug. To treat Paget’s disease of the bone in patients whose alkaline phosphatase level is twice the upper limit of normal or higher and who are symptomatic and at risk for further complications
Adults. 40 mg daily with a full glass of water for 6 mo.
DOSAGE ADJUSTMENT Dosage increased to 10 mg daily for postmenopausal women not receiving estrogen. To increase bone mass in men with osteoporosis
Adults. 10 mg daily or 70 mg once/wk in the morning with a full glass of water at least 30 min before first food, drink, or drug. To treat glucocorticoid-induced osteoporosis in men and women who receive a daily glucocorticoid dosage of 7.5 mg of greater of prednisone and who have low bone mineral density
Adults.5 mg daily in the morning with a full glass of water at least 30 min before first food, drink, or drug. Route Onset Peak Duration P.O. Unknown Unknown 6 wk*

Mechanism of Action

Reduces activity of cells that cause bone loss, slows rate of bone loss after menopause, and increases amount of bone mass. May act by inhibiting osteoclast activity on newly formed bone resorption surfaces, which reduces the number of sites where bone is remodeled. Bone formation then exceeds bone resorption at these remodeling sites, which gradually increases bone mass. May also inhibit bone dissolution by binding to hydroxyapatite crystals, which are composed of calcium, phosphate, and hydroxide and give bone its rigid structure.

Contraindications

Esophageal abnormalities that delay esophageal emptying, such as stricture or achalasia; hypersensitivity to alendronate; hypocalcemia; inability to stand or sit upright for at least 30 minutes

Interactions

antacids, calcium, iron, multivalent cations: Decreased absorption of alendronate aspirin: Increased risk of GI distress any food: Delayed absorption and decreased serum level of alendronate

Side Efect

CNS: Asthenia, dizziness, headache, vertigo
CV: Peripheral edema
GI: Abdominal distention and pain, constialendronate sodium 40 * After single 5-mg dose for osteoporosis; 6 mo after single 5-mg dose for Paget’s disease. pation, diarrhea, dysphagia, esophageal perforation or ulceration, esophagitis, flatulence, gastritis, gastroesophageal reflux disease, heartburn, indigestion, melena, nausea, vomiting
MS: Arthralgia, bone pain, focal osteomalacia, joint swelling, muscle spasms, myalgia
SKIN: Photosensitivity, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Hypocalcemia

Cautions

Monitor patient’s serum calcium level before, during, and after treatment. Expect hypocalcemia to be treated before alendronate therapy. If hypocalcemia occurs during therapy, expect prescriber to order a calcium supplement.

Ensure adequate dietary intake of calcium and vitamin D before, during, and after treatment.
WARNING Alendronate may irritate upper GI mucosa, causing

Side Efect

such as esophageal ulceration. To help minimize these reactions, have patient take drug with a full glass of water and remain upright for at least 30 minutes.

PATIENT SAFTY

Advise patient to take alendronate in the morning with a full glass of water. Explain that beverages such as orange juice, coffee, and mineral water reduce alendronate’s effects.

To help reduce esophageal irritation, tell patient not to chew or suck on tablet.

Instruct patient to wait at least 30 minutes after taking alendronate before eating, drinking, or taking other . Teach patient to remain upright for 30 minutes after taking alendronate and until she has eaten the first food of the day.

Encourage patient to consume adequate daily amounts of calcium and vitamin D.

Category

Chemical class: Tetrahydro-2furancarboxamide hydrochloride
Therapeutic class: Selective alpha1adrenergic antagonist

Pregnancy category: B

Indications

To treat signs and symptoms of benign prostatic hyperplasia
Adults. 10 mg daily taken immediately after same meal each day.

Mechanism of Action

Selectively blocks alpha1-adrenergic receptors in smooth muscle of the bladder neck and prostate, causing relaxation, and blocks postsynaptic alpha1adrenoreceptors in the bladder base and neck, prostate, prostatic capsule, and urethra, preventing further action at these sites. These actions improve urine flow and bladder emptying and reduce urinary hesitancy, frequency, and nocturia.

Contraindications

Hypersensitivity to alfuzosin or its components, moderate or severe hepatic insufficiency, use with CYP3A4 inhibitors, such as itraconazole, ketoconazole, and ritonavir

Interactions

alpha blockers: May potentiate alfuzosin action antihypertensives, nitrates: Possibly synergistic lowering of blood pressure and syncope CYP3A4 inhibitors (such as itraconazole, ketoconazole, ritonavir): Increased alfuzosin effects

Side Efect

CNS: Dizziness, fatigue, headache
CV: Angina, chest pain, edema, orthostatic hypotension, QT-interval prolongation, tachycardia
EENT: Intraoperative floppy iris syndrome, pharyngitis, rhinitis, sinusitis
GI: Abdominal pain, constipation, diarrhea, indigestion, jaundice, hepatotoxicity, nausea
GU: Impotence, priapism
RESP: Bronchitis, upper respiratory tract infection
SKIN: Flushing, pruritus, rash, urticaria
Other: Angioedema, generalized pain

Cautions

Use alfuzosin cautiously in patients who have symptomatic hypotension or who have had a hypotensive response to other . Orthostatic hypotension (with or without symptoms such as dizziness) may occur within hours after alfuzosin administration.

Use cautiously in patients with severe renal insufficiency; decreased drug clearance may increase risk of adverse reactions.

Be aware that alfuzosin shouldn’t be used to treat bladder symptoms in women.

Know that alpha1blockers such as alfuzosin may predispose patients to intraoperative floppy iris syndrome during cataract surgery that may require surgical repair.

Monitor patient for chest pain. If symptoms of angina pectoris occur or worsen, notify prescriber immediately and expect drug to be discontinued.

PATIENT SAFTY

Stress need to take alfuzosin immediately after a meal because absorption is decreased by 50% if taken on an empty stomach.

Tell patient not to crush or chew tablets but to swallow them whole.

Caution patient to avoid hazardous activities until drug’s CNS effects are known and also for several hours after taking dose; blood pressure may drop suddenly after use.

Category

Chemical class: Glucocerebrosidase betaglucosidase
Therapeutic class: Enzyme replacement

Pregnancy category: C

Indications

To treat chronic nonneuropathic Gaucher’s disease in patients with moderate to severe anemia, thrombocytopenia with bleeding tendencies, bone disease, or significant hepatomegaly or splenomegaly
IV: Adults and children age 2 and over. Individualized. 2.5 units/kg to 60 units/kg infused over 1 to 2 hr, usually every 2 wk.
DOSAGE ADJUSTMENT Highly individualized based on body size and disease severity. Some patients may need infusion once every other day; others may need it once every 4 wk. Maintenance dosage progressively reduced every 3 to 6 mo to as low as 1 unit/kg. Route Onset Peak Duration I.V. Up to Unknown Variable 60 min

Mechanism of Action

Catalyzes hydrolysis of glucocerebroside to glucose and ceramide in membrane lipids. Gaucher’s disease results from deficiency of the enzyme beta-glucocerebrosidase and causes the lipid glucocerebroside to accumulate in tissue macrophages.

Contraindications

Hypersensitivity to alglucerase

Side Efect

CNS: Chills, dizziness, fatigue, fever, headache
CV: Transient peripheral edema, vasomotor irritability
EENT: Oral ulcerations
GI: Abdominal discomfort, diarrhea, nausea, vomiting
MS: Backache
Other: I.V. site burning, itching, or swelling

Cautions

Before starting alglucerase therapy, expect to give antihistamines if patient is hypersensitive to drug.

On day of dose, use aseptic technique to dilute alglucerase with normal saline solution to final volume of no more than 200 ml.

Don’t shake drug because doing so could inactivate it.

Don’t use alglucerase if it’s discolored or contains precipitate.

Be aware that drug doesn’t contain preservatives. Discard unused portion.

Infuse drug with in-line I.V. particle filter.

PATIENT SAFTY

Tell patient that he may experience flulike symptoms with each dose of alglucerase.

Instruct patient to report headache, hot flashes, nausea, and other adverse reactions. alglucerase 42

Inform patient that alglucerase is derived from pooled human placental tissue and poses a slight risk of viral contamination.

Advise patient to keep appointments for scheduled doses of alglucerase.

Category

Chemical class: Hemifumarate salt
Therapeutic class: Antihypertensive (direct renin inhibitor)

Pregnancy category: C

(first trimester), D (second and third trimester)

Indications

To treat hypertension
Adults. 150 mg once daily, increased to 300 mg once daily, as needed. Route Onset Peak Duration P.O. Unknown 1–3 hr Unknown

Mechanism of Action

Inhibits renin secreted by the kidneys in response to decreased blood volume and renal perfusion. Renin cleaves angiotensinogen to form angiotensin I, which is converted to angiotensin II by ACE and non-ACE pathways. Angiotension II is a powerful vasoconstrictor that induces release of catecholamines from the adrenal medulla and prejunctional nerve endings. It also promotes aldosterone secretion and sodium reabsorption. Together, these actions increase blood pressure. By inhibiting renin release, aliskiren impairs the renin-angiotensin-aldosterone system. Without the vasoconstrictive effect of angiotension II, blood pressure decreases.

Contraindications

Hypersensitivity to aliskiren or its components; pregnancy; renal impairment, disease, or failure

Interactions

ACE inhibitors (diabetics): Increased risk of hyperkalemia atorvastatin, cyclosporin,
ketoconazole: Increased aliskiren blood level furosemide: Decreased blood furosemide levels irbesartan: Decreased blood aliskiren level

Side Efect

CNS: Dizziness, fatigue, headache, seizures
CV: Hypotension
EENT: Nasopharyngitis
GI: Abdominal pain, diarrhea, dyspepsia, gastroesophageal reflux
GU: Renal calculi
HEME: Decreased hemoglobin and hematocrit
MS: Back pain
RESP: Increased cough, upper respiratory tract infection
SKIN: Rash
Other: Angioedema of head and neck, elevated creatine kinase or uric acid level, gout, hyperkalemia

Cautions

Use cautiously in patients with a history of dialysis or who have moderate to severe renal dysfunction; it isn’t known whether nephritic syndrome and renovascular hypertension are adverse effects of aliskiren.

To prevent hypotension, take measures to correct volume or salt depletion from high-dose diuretic therapy before starting aliskiren. If hypotension occurs during aliskiren therapy, place patient in a supine position and give normal saline solution intravenously, as needed and prescribed.
WARNING Watch closely for angioedema of the head or neck. If angioedema occurs, discontinue aliskiren, notify prescriber, and provide supportive therapy until swelling has ceased. If swelling of the tongue, glottis, or larynx is involved, be prepared to give epinephrine solution 1:1,000 (0.3 ml to 0.5 ml), as prescribed, and provide measures to ensure a patent airway. Be aware that patient shouldn’t receive aliskiren again.

Monitor serum potassium level as ordered in patients who are diabetic and also receiving ACE inhibitor therapy because hyperkalemia may occur. Also monitor serum electrolytes, as ordered, especially in patients wth severe renal impairment.

PATIENT SAFTY

Advise patient to avoid high-fat meals while taking aliskiren because fat decreases drug absorption significantly.

Instruct patient how to monitor blood pressure to determine effectivenss of aliskiren therapy.

Explain that decreased blood pressure could lead to light-headedness, especially in the first few days of therapy. Advise patient to change positions slowly and, if light-headedness develops, to notify prescriber. Tell patient to stop taking aliskiren and to notify prescriber if she faints.

Explain that light-headedness and fainting could also result from dehydration caused by inadequate fluid intake, excessive perspiration, diarrhea, or vomiting.

Instruct patient to avoid using potassium supplements or potassium salt substitutes and to inform all prescribers about her aliskiren and ACE inhibitor therapy.

Stress importance of stopping aliskiren and seeking immediate medical attention if patient has swelling of face, extremities, eyes, lips, or tongue or if patient has trouble swallowing or breathing.

Instruct female patient to notify prescriber immediately if she is or could be pregnant because drug will need to be discontinued and another antihypertensive chosen.

Category

Chemical class: Hypoxanthine derivative, xanthine oxidase inhibitor
Therapeutic class: Antigout

Pregnancy category: C

Indications

To treat gout and hyperuricemia
Adults. 200 to 600 mg daily in divided doses, depending on disease severity. Usual: 200 to 300 mg daily. Maximum: 800 mg daily. To treat secondary hyperuricemia caused by neoplastic disease Children ages 6 to 10. 300 mg daily, adjusted after 48 hr, depending on response to treatment. Children under age 6. 150 mg daily, adjusted after 48 hr, depending on response to treatment. To prevent gout attack
Adults.100 mg daily increased by 100 mg/ wk until serum uric acid level is 6 mg/dl or less. To prevent uric acid nephropathy during vigorous treatment of neoplastic disease
Adults. 600 to 800 mg daily for 2 to 3 days, then adjusted to keep serum uric acid level within normal limits. To treat recurrent calcium oxalate calculi
Adults.200 to 300 mg daily as a single dose or in divided doses, adjusted based on 24hr urine urate level.
DOSAGE ADJUSTMENT For patient with impaired renal function, dosage adjusted to 200 mg daily if creatinine clearance is 10 to 20 ml/min/1.73 m2, 100 mg daily if creatinine clearance is 3 to 10 ml/min/1.73 m2, or 100 mg every other day if creatinine clearance falls below 3 ml/min/1.73 m2. To treat increased serum and urine uric acid levels in patients with leukemia, lymphoma, and solid tumors whose cancer chemotherapy has increased those levels and who can’t tolerate oral therapy
IV:
Adults.200 to 400 mg/m2daily as a single infusion or in equally divided infusions every 6, 8, or 12 hr. Maximum: 600 mg daily. Children.200 mg/m2daily as a single infusion or in equally divided infusions every 6, 8, or 12 hr. Route Onset Peak Duration P.O. 2–3 days 1–3 wk* 1–2 wk

Mechanism of Action

Inhibits uric acid production by inhibiting allopurinol 44 * For hyperuricemia; several months for gout attack prevention. xanthine oxidase, the enzyme that converts hypoxanthine and xanthine to uric acid. Allopurinol is metabolized to oxipurinol, which also inhibits xanthine oxidase.

Incompatibilities

Don’t combine I.V. allopurinol in solution with amikacin, amphotericin B, carmustine, cefotaxime sodium, chlorpromazine hydrochloride, cimetidine hydrochloride, clindamycin phosphate, cytarabine, dacarbazine, daunorubicin hydrochloride, diphenhydramine hydrochloride, doxorubicin hydrochloride, doxycycline hyclate, droperidol, floxuridine, gentamicin sulfate, haloperidol lactate, hydroxyzine hydrochloride, idarubicin hydrochloride, imipenemcilastatin sodium, mechlorethamine hydrochloride, meperidine hydrochloride, metoclopramide hydrochloride, methylprednisolone sodium succinate, minocycline hydrochloride, nalbuphine hydrochloride, netilmicin sulfate, ondansetron hydrochloride, prochlorperazine edisylate, promethazine hydrochloride, sodium bicarbonate, streptozocin, tobramycin sulfate, vinorelbine tartrate.

Contraindications

Hypersensitivity to allopurinol

Interactions

ACE inhibitors: Increased risk of hypersensitivity reactions amoxicillin, ampicillin: Increased risk of rash azathioprine, mercaptopurine: Inactivation of these chlorpropamide: Increased risk of hypoglycemia in patients with renal insufficiency cyclophosphamide, other cytotoxic : Enhanced bone marrow suppression dicumarol: Increased half-life and anticoagulant action of dicumarol thiazide diuretics: Possibly increased risk of allopurinol toxicity uricosuric agents: Increased urinary excretion of uric acid vitamin C (large doses): Possibly urine acidification and increased risk of renal calculus formation

Side Efect

CNS: Chills, drowsiness, fever, headache, neuritis, paresthesia, peripheral neuropathy, somnolence
CV: Vasculitis
EENT: Epistaxis, loss of taste
GI: Abdominal pain, diarrhea, dysphagia, elevated liver function test results, gastritis, granulomatous hepatitis, hepatic necrosis, hepatomegaly, nausea, vomiting
GU: Exacerbated renal calculi, renal failure
HEME: Agranulocytosis, aplastic anemia, bone marrow depression, eosinophilia, leukocytosis, leukopenia, thrombocytopenia
MS: Arthralgia, exacerbation of gout, myopathy
SKIN: Alopecia; ecchymosis; jaundice; maculopapular, scaly, or exfoliative rash (sometimes fatal); pruritus; urticaria

Cautions

As ordered, obtain baseline CBC and uric acid level, and review results of renal and liver function tests before and during allopurinol therapy.

Reconstitute and dilute I.V. preparation to a concentration of 6 mg/ml or less.
WARNING Discontinue allopurinol and notify prescriber immediately at first sign of hypersensitivity reaction, such as rash, which may precede more severe reactions.

To decrease risk of calculus formation, maintain fluid intake of up to 3 L daily and monitor patient for output of 2 L daily. Also, don’t give vitamin C.

PATIENT SAFTY

Advise patient to take allopurinol after meals and to drink at least 10 large glasses of water daily.

Instruct patient to report unusual bleeding or bruising, fever, chills, gout attack, numbness, and tingling.

Inform patient that acute gout attacks may occur more often early in allopurinol treatment and that results may not be noticeable for 2 weeks or longer.

Instruct patient not to drive or perform hazardous tasks if drug causes drowsiness.

Category

Chemical class: Selective 5-hydroxytryptamine1(5-HT1) receptor agonist
Therapeutic class: Antimigraine drug

Pregnancy category: C

Indications

To treat acute migraine Adults and adolescents ages 12 to 17. Initial: 6.25 to 12.5 mg as a single dose, repeated in 2 hr p.r.n. Maximum: 2 doses/ 24 hr or 4 migraine treatments/mo.
DOSAGE ADJUSTMENT For patient with impaired renal or hepatic function, initial dose reduced to 6.25 mg with maximum daily dose of 12.5 mg.

Mechanism of Action

May stimulate 5-HT1receptors on intracranial blood vessels and sensory nerves in trigeminal vascular system. By activating these receptors, almotriptan selectively constricts inflamed and dilated cranial blood vessels and inhibits production of proinflammatory neuropeptides. It also interrupts transmission of pain signals to the brain.

Contraindications

Basilar or hemiplegic migraine; cerebrovascular, peripheral vascular, or ischemic or vasospastic coronary artery disease (CAD); hypersensitivity to almotriptan or its components; hypertension (uncontrolled); use within 24 hours of other serotonin-receptor agonists or ergotamine-containing or ergottype

Interactions

ergotamine-containing : Prolonged vasospastic reactions erythromycin, itraconazole, ketoconazole, ritonavir: Possibly increased blood almotriptan level MAO inhibitors, verapamil: Increased blood almotriptan level selective serotonin reuptake inhibitors, such as citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline: Increased risk of serotonin syndrome serotonin norepinephrine reuptake inhibitors, such as duloxetine, venlafaxine: Increased risk of serotonin syndrome

Side Efect

CNS: Dizziness, headache, paresthesia, seizures, somnolence, syncope
CV: Coronary artery vasospasm, hypertension, ischemia, MI, palpitations, vasodilation, ventricular fibrillation, ventricular tachycardia
EENT: Dry mouth
GI: Nausea
Other: Serotonin syndrome

Cautions

WARNING Because almotriptan can cause coronary artery vasospasm, monitor patient with CAD for angina. Because it may cause peripheral vasospastic reactions, such as ischemic bowel disease, watch for abdominal pain and bloody diarrhea.

For patient with risk factors for CAD but no known cardiovascular abnormalities, expect to give first dose of almotriptan in a medical facility.

In patient with risk factors for CAD, obtain an ECG immediately after first dose of almotriptan, as ordered, because cardiac ischemia can occur without causing clinical symptoms.

Expect to give a lower dosage to patients with hepatic or renal dysfunction because of impaired drug metabolism or excretion.

Monitor blood pressure regularly during therapy in patients with hypertension because almotriptan may produce a transient increase in blood pressure.
WARNING Monitor patient for evidence of serotonin syndrome, such as agitation, chills, confusion, diaphoresis, diarrhea, fever, hyperactive reflexes, poor coordination, restlessness, shaking, talking or acting with uncontrolled excitement, tremor, and twitching. In its most severe form, serotonin syndrome can resemble neuroleptic malignant syndrome, which includes a high fever, muscle rigidity, autonomic instability with possible fluctuations in vital signs, and mental status changes.

Monitor patients hypersensitive to sulfonamides for hypersensitivity to almotriptan because cross-sensitivity may occur.

PATIENT SAFTY

Inform patient that almotriptan is used to treat acute migraine and that he shouldn’t take it to treat nonmigraine headaches.

Advise patient to consult prescriber before taking any OTC or prescription .

Advise patient not to take more than maximum prescribed.

Caution patient that drug may cause adverse CNS reactions, and advise him to avoid hazardous activities until he knows how drug affects him.

Instruct patient to seek emergency care almotriptan malate 46 immediately for cardiac symptoms (such as heaviness, pain, pressure, or tightness in chest, jaw, neck, or throat) or if multiple new symptoms develop (such as mental changes, high fever, incoordination, nausea, vomiting, diarrhea) after taking drug.

Category

Chemical class: Selective serotonin 5-HT3 receptor antagonist
Therapeutic class: Antidiarrheal

Pregnancy category: B

Indications

To treat women with severe diarrhea predominant irritable bowel syndrome (IBS) who haven’t responded to conventional therapy
Adults. Initial: 1 mg daily for 4 wk, increased to 1 mg b.i.d. if needed. Discontinued if no response in first 4 wk of therapy or if drug doesn’t adequately control symptoms after 4 wk of b.i.d. regimen.

Mechanism of Action

Inhibits activation of 5-HT3nonselective cation channels found in enteric neurons in the GI tract, thereby decreasing visceral sensations, colonic transit, and secretions in the GI tract. These changes reduce GI pain and hyperactivity, symptoms that are prominent in diarrhea-predominant IBS.

Contraindications

Administration with fluvoxamine, history of chronic or severe constipation or sequelae from constipation, Crohn’s disease, diverticulitis, GI perforation or adhesions, hypercoagulable state, impaired intestinal circulation, intestinal obstruction or stricture, ischemic colitis, thrombophlebitis, toxic megacolon, or ulcerative colitis; hypersensitivity to alosetron or its components; severe hepatic impairment

Interactions

fluvoxamine,
ketoconazole: Increased blood alosetron level cimetidine, clarithromycin, itraconazole, protease inhibitors, quinolones, telithromycin, voriconazole: Possibly increased alosetron level

Side Efect

CNS: Anxiety, fatigue, headache, hypnagogic effects, malaise, temperature regulation disturbances
CV: Tachyarrhythmias
GI: Abdominal or GI discomfort and pain, abdominal distention, constipation (may be severe), diarrhea, dyspepsia, flatulence, GI spasms or lesions, hemorrhoids, hemorrhoidal hemorrhage, hyposalivation, ileus, impaction, ischemic colitis, nausea, obstruction, perforation, regurgitation and reflux, small-bowel mesenteric ischemia, ulceration
GU: Urinary frequency
RESP: Breathing disorders
SKIN: Diaphoresis, rash, urticaria
Other: Nonspecific cramps or pain

Cautions

Be aware that only physicians enrolled in GlaxoSmithKline’s prescribing program for alosetron should prescribe the drug and only patients who have read and signed the patient-physician agreement can receive the drug. Confirm that the agreement has been signed before therapy starts.

Use alosetron cautiously in patients with mild to moderate liver dysfunction because alosetron is extensively metabolized in the liver.

Report all

Side Efect

to alosetron to the prescriber and to Prometheus at 1-888-423-5227.
WARNING Monitor patient for constipation, especially if she’s elderly or debilitated or takes that decrease GI motility. Also watch for evidence of ischemic colitis, such as rectal bleeding, bloody diarrhea, or new or worsening abdominal pain. Serious adverse GI reactions may occur without
WARNING. If they do, be prepared to stop alosetron therapy immediately. If discontinued for ischemic colitis, drug shouldn’t be resumed later; however, a patient who no longer has constipation can resume it, if needed.

Make sure program stickers required by drug maker are affixed to all prescriptions,including refills, before giving to patient.

PATIENT SAFTY

Explain that alosetron therapy can’t begin until patient has read the medication guide that outlines drug’s risks and benefits and has signed the permission form.

Instruct patient not to start alosetron if constipated and to notify prescriber.

Advise patient that serious adverse GI effects may occur without
WARNING. Tell her to stop taking alosetron immediately and to notify prescriber if evidence of ischemic colitis or constipation arises. Tell her to notify prescriber if constipation doesn’t resolve after stopping drug.

Inform patient that alosetron will be stopped after 4 weeks of 1 mg b.i.d. if it dosen’t control IBS symptoms.

Category

Chemical class: Plasma protein
Therapeutic class: Enzyme replacement

Pregnancy category: C

Indications

To treat congenital alpha1-antitrypsin deficiency in patients with signs of panacinar emphysema (Prolastin); to augment and maintain patients with emphysema who are deficient in alpha1proteinase inhibitor
IV:
Adults. 60 mg/kg infused over 30 min (Prolastin) or 15 min (Prolastin-C, Zemaira) at a rate of at least 0.08 ml/kg/ min once weekly.

Mechanism of Action

Replaces the enzyme alpha1-antitrypsin, which normally inhibits the proteolytic enzyme elastase in patients with alpha1antitrypsin deficiency. Without alpha1proteinase inhibitor, elastase attacks and destroys alveolar membranes and causes emphysema.

Contraindications

Hypersensitivity to alpha1-proteinase inhibitor, its components, or other alpha1proteinase products; selective immunoglobulin A (IgA) deficiency in patients with anti-IgA antibodies

Interactions

smoking: Inactivation of alpha1-proteinase inhibitor

Side Efect

CNS: Asthenia, chills, dizziness, fever, headache, light-headedness, malaise, paresthesia
EENT: Sinusitis
ENDO: Hot flashes
HEME: Mild, transient leukocytosis
RESP: Upper respiratory tract infection, worsening of existing COPD
SKIN: Pruritus, rash
Other: Flulike symptoms, infusion site pain

Cautions

Use alpha1-proteinase inhibitor cautiously in patients at risk for circulatory overload because drug is a colloid solution that increases plasma volume.

Before reconstituting, remove drug and diluent from refrigerator and let it warm to room temperature.

To reconstitute, remove caps from vials and clean rubber stoppers with antiseptic. After stoppers are dry, remove protective cover from diluent end of transfer device and insert into center of upright diluent vial. Then remove protective cover from drug end of transfer device, invert diluent vial with attached transfer device, and using minimal force, insert drug end of transfer device into center of rubber stopper of upright drug vial. Make sure flange of transfer device rests on stopper surface so that diluent flows into drug vial.

During diluent transfer, wet lyophilized cake completely by gently tilting drug vial. Don’t let air inlet filter face downward. (Take care not to lose the vacuum because this will prolong drug reconstitution.) Once diluent transfer is complete, pull transfer device along with attached diluent vial out of drug vial and discard. Gently swirl drug vial until powder is completely dissolved. Avoid shaking because this may cause drug to foam and degrade.

If more than one vial of alpha1-proteinase inhibitor is required, use aseptic technique to transfer reconstituted solution from alpha1-proteinase inhibitor (human) 48 each vial into a sterile I.V. administration container.

Administer at room temperature within 3 hours of reconstitution as an I.V. infusion, using the large-volume 5-micron conical filter provided. Place filter between distal end of I.V. administration set and infusion set, and infuse at 0.08 ml/kg/min or as determined by patient response and comfort.
WARNING Alpha1-proteinase inhibitor is made from human plasma and may contain infectious agents, such as viruses. Make sure patient is immunized against hepatitis B before giving drug. If time doesn’t allow for antibody formation, give a single dose of hepatitis B immune globulin with hepatitis B vaccine, as prescribed.

Monitor patient for delayed fever, which may occur up to 12 hours after therapy. Fever usually resolves within 24 hours.

PATIENT SAFTY

Tell patient to report immediately early evidence of allergic reaction, such as chest tightness, trouble breathing, faintness, hives, wheezing, and any other unusual symptoms.

Advise patient to notify prescriber about signs or symptoms of viral infection (chills, drowsiness, fever, and runny nose, followed 2 weeks later by joint pain and a rash) after receiving drug.

Stress importance of receiving weekly doses to maintain an adequate antielastase barrier in the lungs. Explain that treatment must continue for life.

Warn patient not to smoke. alprazolam Apo-Alpraz (CAN),Novo-Alprazol (CAN),Nu-Alpraz,Xanax,Xanax XR Chemical class: Benzodiazepine
Therapeutic class: Antianxiety drug

Pregnancy category: D

Controlled substance schedule: IV

Indications

To control anxiety disorders, relieve anxiety (short-term therapy), or treat anxiety associated with depression
Adults. Initial: 0.25 to 0.5 mg t.i.d., adjusted to patient’s needs. Maximum: 4 mg daily in divided doses.
DOSAGE ADJUSTMENT In elderly or debilitated patients or patients with advanced hepatic disease, initial dosage 0.25 mg b.i.d. or t.i.d. and increased gradually, as needed and tolerated. To treat panic attack ORALLY
,
Adults. Initial: 0.5 mg t.i.d., increased every 3 to 4 days by no more than 1 mg daily, based on patient response. Maximum: 10 mg daily in divided doses.
Adults.Initial: 0.5 to 1 mg daily in morning, increased every 3 to 4 days by no more than 1 mg daily, based on patient response. Maximum: 10 mg daily as single dose in morning.

Mechanism of Action

May increase effects of gamma-aminobutyric acid (GABA) and other inhibitory neurotransmitters by binding to specific benzodiazepine receptors in limbic and cortical areas of the CNS. GABA inhibits excitatory stimulation, which helps control emotional behavior. The limbic system contains many benzodiazepine receptors, which may help explain drug’s antianxiety effects.

Contraindications

Acute angle-closure glaucoma; hypersensitivity to alprazolam, its components, or other benzodiazepines; itraconazole or ketoconazole therapy

Interactions

antacids: Altered alprazolam absorption rate cimetidine, disulfiram, fluoxetine, isoniazid, metoprolol, oral contraceptives, propoxyphene, propranolol,
valproic acid: Decreased alprazolam elimination and increased effects
CNS depressants: Possibly increased CNS effects of both digoxin: Possibly increased serum digoxin level, causing digitalis toxicity itraconazole,
ketoconazole: Possibly profoundly inhibited alprazolam metabolism levodopa: Decreased effects of levodopa neuromuscular blockers: Possibly potentiated or antagonized effects of these
phenytoin: Possibly increased serum level, causing phenytoin toxicity probenecid: Possibly faster onset or prolonged effects of alprazolam ranitidine: Possibly reduced absorption of alprazolam
alcohol use: Enhanced adverse CNS effects of alprazolam

Side Efect

CNS: Agitation, akathisia, confusion, depression, dizziness, drowsiness, fatigue, hallucinations, headache, insomnia, irritability, lack of coordination, lightheadedness, memory loss, nervousness, paresthesia, rigidity, speech problems, syncope, tremor, weakness
CV: Chest pain, edema, hypotension, nonspecific ECG changes, palpitations, tachycardia
EENT: Blurred vision, altered salivation, dry mouth, nasal congestion, tinnitus
ENDO: Galactorrhea, gynecomastia, hyperprolactinemia
GI: Abdominal discomfort, anorexia, constipation, diarrhea, elevated liver function test results, hepatitis, hepatic failure, nausea, vomiting
GU: Altered libido, urinary hesitancy
MS: Dysarthria, muscle rigidity and spasms
RESP: Hyperventilation, upper respiratory tract infection
SKIN: Dermatitis, diaphoresis, pruritus, rash, Stevens-Johnson syndrome
Other: Weight gain or loss

Cautions

Expect to give a higher dosage if patient’s panic attacks occur unexpectedly or during such activities as driving.

Because use can lead to dependency, expect to reduce dosage gradually when stopping drug. To prevent withdrawal symptoms, don’t stop drug abruptly.

PATIENT SAFTY

Warn against stopping drug abruptly because withdrawal symptoms may occur.

Instruct patient never to increase prescribed dose because of risk of dependency.

Urge patient to avoid drinking alcohol during alprazolam therapy.

Advise patient to avoid driving and activities that require alertness until alprazolam’s effects are known.

Instruct female patient of childbearing age to notify prescriber immediately if she becomes or might be pregnant. Drug isn’t recommended during pregnancy.

Category

Chemical class: Prostaglandin E1
Therapeutic class: Anti-impotence drug

Pregnancy category: C

Indications

To treat erectile dysfunction caused by vascular or psychogenic causes or both INTRACAVERNOUS INJECTION(CAVERJECT, EDEX)
Adults. Initial: 2.5 mcg. Increased to 5 mcg if partial response or 7.5 mcg if no response, followed by incremental increases of 5 to 10 mcg until erection suitable for intercourse (not exceeding 1-hr duration) is achieved. No more than 2 doses, separated by 1 hr, should be given on a single day during initial titration phase. Maximum: 3 doses/wk, separated by 24 hr. URETHRAL SUPPOSITORY(MUSE)
Adults. Initial: 125 to 250 mcg. If no response, dosage increased in increments to 500 or 1,000 mcg until erection suitable for intercourse (not exceeding 1-hr duration) is achieved. Maximum: 2 doses/24 hr. To treat erectile dysfunction caused by spinal cord injury INTRACAVERNOUS INJECTION(CAVERJECT, EDEX)
Adults.Initial: 1.25 mcg. Increased to 2.5 mcg if partial response, then to 5 mcg, and increased in 5-mcg increments until erection suitable for intercourse (not exceeding 1-hr duration) is achieved. No more than 2 doses, separated by 1 hr, should be given on a single day during initial titration phase. Maximum: 3 doses/ week, separated by 24 hr. Route Onset Peak Duration Intra5–20 min Unknown 60 min cavernous Intra5–10 min Unknown 30–60 min urethral

Contraindications

Anuria, balanitis (inflammation of head of alprostadil 50 penis), cavernosal fibrosis, hypersensitivity to alprostadil or its components, hyperviscosity syndrome, indwelling urethral catheter, leukemia, men for whom sexual activity is contraindicated, multiple myeloma, penile angulation, penile implants, Peyronie’s disease, polycythemia, severe hypospadius (urethral opening on underside of penis), sickle cell anemia or trait, tendency to develop venous thrombosis, thrombocythemia, urethral obstruction or stricture, urethritis

Interactions

anticoagulants: Possibly increased risk of bleeding cyclosporine: Possibly decreased blood cyclosporine level

Side Efect

CNS: Dizziness, headache, syncope
CV: Hypertension, hypotension, tachycardia, vasodilation
EENT: Nasal congestion, sinusitis
GU: Pelvic pain; penile disorders, including edema, fibrosis, pain, and rash; priapism; prolonged erection; prostatic pain or enlargement; urethral abrasions; urethral bleeding
MS: Back pain
RESP: Cough, upper respiratory tract infection
Other: Flulike symptoms, injection site bruising or hematoma, needle breakage

Cautions

Reconstitute solution with 1 ml diluent, for a concentration of 5, 10, 20, or 40 mcg/ ml, depending on vial strength. Gently swirl contents of reconstituted vial. Use reconstituted solution within 24 hours when stored at room temperature. Don’t use vials that contain precipitate or discolored solution. Discard unused reconstituted solution.

Using a 1⁄2-inch 27G to 30G needle, inject drug at a 90-degree angle into proximal third of spongy tissue that runs the length of the dorsolateral aspect of penis, avoiding any visible veins. Rotate injection sites by alternating sides of the penis.Dorsal veins Outside caverno Inside co Dorsal artery Corpus cavernosum Urethra Trabecular smooth muscles Lacunar space Transverse section of penis Dorsal veins Alprostadil Receptor Adenyl cyclase Outside corpus cavernosum cell Inside corpus cavernosum cell ATP cAMP Protein kinase Dorsal artery Corpus cavernosum Urethra Trabecular smooth muscles Lacunar space Transverse section of penis Alprostadil causes penile erection by increasing blood flow to the penis through relaxation of trabecular smooth muscles and dilation of cavernosal arteries (upper right). A naturally occurring prostaglandin, alprostadil interacts with specific membrane-bound receptors in the corpora cavernosa cells of the penis. This action activates intracellular adenyl cyclase (lower right), which in turn converts adenosine triphosphate (ATP) into cyclic adenosine monophosphate (cAMP). Increased intracellular levels of cAMP activate protein kinase, an enzyme that activates other enzymes to initiate a cascade of chemical reactions. These chemical reactions cause the trabecular smooth muscles to relax and the cavernosal arteries to dilate. Blood flow to the penis is then increased, which distends the penile lacunar spaces and compresses the veins, trapping blood in the penis and causing it to become enlarged and rigid.

Mechanism of Action

Carefully examine penis for evidence of penile fibrosis. Expect to discontinue treatment if patient develops cavernosal fibrosis, penile angulation, or Peyronie’s disease (hardening of the corpora cavernosa, which causes penis to become distorted when erect) during therapy.
WARNING Watch for prolonged erection after giving drug. Notify prescriber, and be prepared to treat patient for priapism if erection lasts longer than 4 hours.

If patient is receiving an anticoagulant, such as warfarin or heparin, watch for bleeding at injection site because drug may inhibit platelet aggregation.

PATIENT SAFTY

Inform patient that initial therapy must be performed in the office setting. Teach him how to correctly administer intracavernous injections or urethral suppositories. Inform him that the goal of treatment is to produce an erection that lasts no longer than 1 hour.

Advise patient to use alprostadil for injection no more than three times/week and to separate doses by 24 hours. Inform patient using urethral suppositories not to exceed two doses in a 24-hour period.

Tell patient to inform prescriber immediately about nodules or hard tissue in the penis; an erection that persists for more than 4 hours; new or worsened penile pain; or persistent curvature, redness, swelling, or tenderness of the erect penis.

Inform patient that common adverse reactions include mild to moderate pain immediately after injection and burning after suppository insertion. Also, needle may break. Advise patient to avoid it by following prescriber’s instructions exactly and by handling injection device properly. If needle breaks during injection and he can see and grasp broken end, he should remove it and contact prescriber. If he can’t see or grasp broken end, he should seek medical care.

Instruct patient using suppository form to urinate just before inserting suppository and to insert it with applicator supplied with drug. Tell patient to hold penis upright after insertion and to roll it firmly between his hands to distribute drug.

Tell patient to sit, stand, or walk for 10 minutes after inserting suppository to increase blood flow and enhance erection.

Tell patient to expect an erection 5 to 20 minutes after injecting drug or about 10 minutes after inserting suppository.

Advise patient not to change dosage without consulting prescriber and to keep scheduled follow-up appointments.

Warn patient that alprostadil offers no protection from sexually transmitted diseases. Urge him to use a condom to decrease risk of blood-borne disease, because injection can cause minor bleeding at injection site.

Instruct patient not to reuse or share needles or syringes. Inform him of proper procedure for sharps disposal.

Warn patient using suppository form not to have sexual intercourse with a pregnant woman unless a condom is used because drug’s effect on pregnancy is unknown.

Advise patient who plans to travel not to check drug with airline baggage or store it in a closed car.

Category

Chemical class: Purified glycoprotein
Therapeutic class: Thrombolytic

Pregnancy category: C

Indications

To treat acute MI ACCELERATED
IV: Adults weighing more than 67 kg (148 lb). 15-mg bolus followed by 50 mg infused over next 30 min and then by 35 mg infused over next 60 min. Adults weighing 67 kg or less. 15-mg bolus followed by 0.75 mg/kg (up to 50 mg) infused over next 30 min and then 0.5 mg/ kg (up to 35 mg) infused over next 60 min.
IV: Adults weighing more than 65 kg (143 lb). 100 mg infused over 3 hr as follows: 6 to 10 mg by bolus over first 1 to 2 min, 50 to 54 mg over remainder of first hr, 20 mg over second hr, and 20 mg over third hr. Adults weighing 65 kg or less. 1.25 mg/kg alteplase 52 infused over 3 hr on similar schedule as those weighing more than 65 kg. To treat acute ischemic stroke To avoid acute bleeding complications, treatment for acute ischemic stroke must begin within 3 hr after onset of stroke symptoms and only after computed tomography or other diagnostic imaging method excludes intracranial hemorrhage.
IV:
Adults. 0.9 mg/kg infused over 60 min, with 10% of total dose given as bolus over first min. Maximum: 90 mg. To treat pulmonary embolism
IV:
Adults. 100 mg infused over 2 hr. Route Onset Peak Duration I.V. Immediate 20–120 min 4 hr

Mechanism of Action

Binds to fibrin in a thrombus and converts trapped plasminogen to plasmin. Plasmin breaks down fibrin, fibrinogen, and other clotting factors, which dissolves the thrombus.

Incompatibilities

Don’t add other to solution that contains alteplase.

Contraindications

For all indications: Active internal bleeding, arteriovenous malformation or aneurysm, bleeding diathesis, intracranial neoplasm, severe uncontrolled hypertension For acute MI and pulmonary embolism only: History of stroke, intracranial or intraspinal surgery or trauma in past 2 months For acute ischemic stroke only: Recent head trauma, recent intracranial surgery, recent stroke, seizure activity at onset of stroke, subarachnoid hemorrhage, suspicion or history of intracranial hemorrhage

Interactions

that alter platelet function, such as abciximab, acetylsalicylic acid, and dipyridamole; heparin; vitamin K antagonists: Increased risk of bleeding

Side Efect

CNS: Cerebral edema, cerebral herniation, fever, seizure, stroke
CV: Arrhythmias (including bradycardia and electromechanical dissociation), cardiac arrest, cardiac tamponade, cardiogenic shock, cholesterol embolism, coronary thrombolysis, heart failure, hypotension, mitral insufficiency, myocardial reinfarction or rupture, pericardial effusion, pericarditis, venous thrombosis and embolism
EENT: Epistaxis, gingival bleeding, laryngeal edema
GI: GI bleeding, nausea, retroperitoneal bleeding, vomiting
GU: GU bleeding
RESP: Pleural effusion, pulmonary edema, pulmonary reembolization
SKIN: Bleeding at puncture sites, ecchymosis, rash, urticaria
Other: Anaphylaxis

Cautions

WARNING To avoid acute bleeding complications, treatment for acute ischemic stroke must begin within 3 hr after onset of stroke symptoms and only after computed tomography or other diagnostic imaging method excludes intracranial hemorrhage.

Immediately before use, reconstitute alteplase with sterile water for injection only. Swirl gently to dissolve powder; don’t shake.

Monitor patient for bleeding, especially at arterial puncture sites.

Monitor blood pressure and heart rate and rhythm frequently during and after therapy.
WARNING Alteplase therapy may cause arrhythmias from sudden reperfusion of the myocardium. Monitor continuous ECG for arrhythmias during drug therapy.

Minimize bleeding from noncompressible sites by avoiding internal jugular and subclavian venous puncture sites.

Discontinue alteplase immediately if serious bleeding occurs.

After administering alteplase, apply pressure for at least 30 minutes, followed by a pressure dressing.

Store reconstituted solution at room temperature (about 86° F [30° C]) or refrigerated (36° to 46° F [2.2° to 7.7° C]).

PATIENT SAFTY

Tell patient to immediately report bleeding, including from the nose or gums.

Advise patient to limit physical activity during alteplase administration to reduce risk of injury and bleeding.

Category

Chemical: Aluminum salt Therapeutic: Antacid, phosphate binder

Pregnancy category: Not rated

Indications

To treat hyperacidity associated with gastric hyperacidity, gastritis, hiatal hernia, peptic esophagitis, and peptic ulcers; to prevent phosphate renal calculus formation; to reduce hyperphosphatemia in chronic renal failure ALUMINUM CARBONATE ,SUSPENSION,
Adults.2 capsules or tablets or 10 ml suspension every 2 hr up to 12 times daily p.r.n. ALUMINUM HYDROXIDE , SUSPENSION,
Adults.500 to 1,500 mg as capsules or tablets in divided doses 3 to 6 times daily, taken between meals and at bedtime; 5 to 30 ml as suspension, p.r.n., taken between meals and at bedtime. Route Onset Peak Duration P.O. Varies Unknown 20–40 min*

Mechanism of Action

Neutralizes or reduces gastric acidity, increasing stomach and duodenal alkalinity. Protects stomach and duodenum lining by inhibiting pepsin’s proteolytic activity. Binds with phosphate ions in intestine to form insoluble aluminum-phosphate compounds, which lower blood phosphate level.

Contraindications

Hypersensitivity to aluminum

Interactions

allopurinol, chloroquine, corticosteroids, diflunisal, digoxin, ethambutol, H2-receptor blockers, iron, isoniazid, penicillamine, phenothiazines, ranitidine, tetracyclines, thyroid hormones, ticlopidine: Decreased effects of these benzodiazepines: Increased benzodiazepine effects

Side Efect

CNS: Encephalopathy
GI: Constipation, intestinal obstruction, white-speckled stool
MS: Osteomalacia, osteoporosis
Other: Aluminum accumulation in serum, bone, and CNS; aluminum intoxication; electrolyte imbalances

Cautions

Don’t give aluminum hydroxide within 1 to 2 hours of other oral .

Know that two 0.6-g aluminum hydroxide tablets can neutralize 16 mEq of acid.

Monitor patient’s serum levels of sodium, phosphate, and other electrolytes, as appropriate.

PATIENT SAFTY

Instruct patient to chew tablets thoroughly before swallowing and then to drink a full glass of water.

Warn patient not to take maximum dosage for more than 2 weeks unless prescribed because doing so may cause stomach to secrete excess hydrochloric acid.

Teach patient to prevent constipation with a high-fiber diet and increased fluid intake (2 to 3 L daily), if appropriate.

If patient takes other prescription , advise him to notify prescriber about thembefore taking aluminum because of risk of interactions.

Advise patient to notify prescriber if symptoms worsen or don’t subside.

Category

Chemical class: Single stereoisomer aluminum;alvimopan 54 * If fasting; at least 3 hr if given 1 hr after meals.
Therapeutic class: Mu opioid receptor antagonist

Pregnancy category: B

Indications

To accelerate GI recovery in hospitalized patients after partial largeor smallbowel resection with primary anastomosis
Adults.Initial: 12 mg started 30 min to 5 hr before surgery, followed by 12 mg b.i.d. starting the day after surgery for up to 7 days or until discharge. Maximum: 24 mg/ day with a maximum of 15 doses total. Route Onset Peak Duration P.O. Unknown 2 hr Unknown

Mechanism of Action

Competitively binds to selective mu opioid receptors in GI tract, antagonizing peripheral effects of opioids on GI motility and secretion without reversing the central analgesic effects of opioid agonists. This action alleviates postoperative ileus by causing bowel function to return more quickly after part of bowel has been removed and an end-to-end anastomosis performed.

Contraindications

Hypersensitivity to alvimopan or its components, severe hepatic or renal impairment, use of opiods for more than 7 consecutive days immediately before alvimopan starts

Interactions

opioids given within previous 7 days at therapeutic doses: Increased sensitivity to alvimopan

Side Efect

GI: Abdominal pain, constipation, diarrhea, dyspepsia, flatulence
GU: Urine retention
HEME: Anemia
MS: Back pain
Other: Hypokalemia

Cautions

Don’t give alvimopan to patients with severe hepatic or renal impairment or to patients having surgery to correct a complete bowel obstruction.

Alvimopan is prescribed only for shortterm use with maximum of 15 doses and is only dispensed in hospitals enrolled in Entereg Access Support and Education (E.A.S.E.) program. Closely monitor number of doses given, and expect to stop drug when patient has received 15 doses or is discharged from hospital.

Monitor patient’s serum potassium level closely, as ordered, because drug may cause hypokalemia. Also check patient’s hemoglobin level and hematocrit because drug has been associated with anemia.

Monitor patient with mild to moderate hepatic or renal failure for evidence of high alvimopan levels, such as abdominal pain or cramping, diarrhea, nausea, and vomiting. If present, alert prescriber.

Monitor Japanese patients closely for possible adverse effects because alvimopan level may be higher in this population.

PATIENT SAFTY

Explain the need to accurately describe long-term or intermittent use of opioid pain therapy, including any use of opioids in the week before receiving alvimopan. Taking almivopan after such use may cause serious adverse GI reactions.

Inform patient that the most common adverse effects of alvimopan are constipation, dyspepsia, and flatulence.

Tell patient that drug is for in-hospital use only and will not be taken at home.

Category

Chemical class: Adamantane derivative
Therapeutic class: Antidyskinetic, antiviral

Pregnancy category: C

Indications

To manage symptoms of primary Parkinson’s disease, postencephalitic parkinsonism, arteriosclerotic parkinsonism, and parkinsonism caused by CNS injury from carbon monoxide intoxication , SYRUP,
Adults. Initial: 100 mg b.i.d. Maximum: 400 mg daily in divided doses. To treat drug-induced extrapyramidal reactions , SYRUP,
Adults. Initial: 100 mg b.i.d. Maximum: 300 mg daily in divided doses.
DOSAGE ADJUSTMENT For elderly patients, patients taking high doses of other antidyskinetics, and patients who have a serious medical condition (such as heart failure, epilepsy, or psychosis), initial dosage reduced to 100 mg daily, with gradual titration to 100 mg b.i.d. after 1 to several wk. For patients with impaired renal function, dosage adjusted to 200 mg on day 1 and then to 100 mg daily if creatinine clearance is 30 to 50 ml/min/1.73 m2; to 200 mg on day 1 and then to 100 mg every other day if creatinine clearance is 15 to 29 ml/min/ 1.73 m2; and to 200 mg every wk if creatinine clearance is less than 15 ml/min/1.73 m2or if patient is receiving hemodialysis. To prevent and treat respiratory tract infection caused by influenza A , SYRUP, Adults and children age 12 and over. Initial: 200 mg daily or 100 mg b.i.d. Maximum: 200 mg daily.
DOSAGE ADJUSTMENT In impaired renal function, if creatinine clearance is 30 to 50 ml/min/1.73 m2, 200 mg on day 1 and then 100 mg daily. If clearance is 15 to 29 ml/min/1.73 m2, 200 mg on day 1 and then 100 mg every other day. If clearance is less than 15 ml/min/1.73 m2or patient is having hemodialysis, 200 mg every wk. Children ages 9 to 12. 100 mg every 12 hr. Maximum: 200 mg daily. Children ages 1 to 9. 1.5 to 3 mg/kg every 8 hr or 2.2 to 4.4 mg/kg every 12 hr. Maximum: 150 mg/day. Route Onset Peak Duration P.O. In 48 hr* Unknown Unknown

Mechanism of Action

Affects dopamine, a neurotransmitter that is synthesized and released by neurons leading from substantia nigra to basal ganglia and is essential for normal motor function. In Parkinson’s disease, progressive degeneration of these neurons reduces intrasynaptic dopamine. Amantadine may cause dopamine to accumulate in the basal ganglia by increasing dopamine release or by blocking dopamine reuptake into the presynaptic neurons of the CNS. Amantadine also may stimulate dopamine receptors or make postsynaptic receptors more sensitive to dopamine. These actions help control alterations in involuntary muscle movements, such as tremors and rigidity, that are associated with Parkinson’s disease. Amantadine may inhibit influenza A viral replication by blocking uncoating of virus and release of viral nucleic acid into respiratory epithelial cells. It also may interfere with early replication of viruses that have already penetrated cells.

Contraindications

Angle-closure glaucoma, hypersensitivity to amantadine or its components

Interactions

anticholinergics or other with anticholinergic activity, other antidyskinetics, antihistamines, phenothiazines, tricyclic antidepressants: Possibly increased anticholinergic effects and risk of paralytic ileus carbidopa-levodopa, levodopa: Increased effectiveness of these CNS stimulants: Excessive CNS stimulation, possibly causing arrhythmias, insomnia, irritability, nervousness, or seizures hydrochlorothiazide, triamterene: Possibly decreased amantadine clearance and increased risk of toxicity live-virus vaccines: Possibly interference with vaccine effectiveness quinidine, quinine, trimethoprimsulfamethoxazole: Increased blood amantadine level
alcohol use: Possibly increased risk of CNS effects—including confusion, dizziness, and light-headedness—and orthostatic hypotension

Side Efect

CNS: Agitation, anxiety, confusion, dizziness, drowsiness, fatigue, fever, hallucinations, insomnia, irritability, light-headedamantadine hydrochloride 56 * Antidyskinetic action; antiviral action unknown. ness, mental impairment, nervousness, neuroleptic malignant syndrome, nightmares, suicidal ideation, syncope
CV: Arrhythmias, cardiac arrest, orthostatic hypotension, peripheral edema, tachycardia
EENT: Blurred vision; dry mouth, nose, or throat; keratitis; mydriasis
GI: Constipation, diarrhea, dysphagia, nausea
GU: Dysuria, increased libido
HEME: Agranulocytosis, leukopenia, neutropenia
RESP: Acute respiratory failure, pulmonary edema, tachypnea
SKIN: Diaphoresis, livedo reticularis (purplish, netlike rash), pruritus
Other: Anaphylaxis; intense urges to perform certain activities, such as gambling or sexual acts

Cautions

Be aware that prophylactic therapy with amantadine should begin as soon as possible after exposure to persons infected with influenza A virus and should continue for 10 days. During an influenza epidemic, expect drug to be given daily throughout the epidemic, which typically lasts 6 to 8 weeks. If patient has previously received inactivated influenza A vaccine, prescriber may discontinue it when sure that patient has developed active immunity against the virus. If patient receives inactivated influenza A vaccine at the same time amantadine therapy starts, expect amantadine to be given for 2 to 3 weeks.

Expect amantadine therapy to start 24 to 48 hours after the onset of influenza A symptoms and to continue 48 hours after they resolve.

Monitor patients who have a history of psychiatric illness or substance abuse because amantadine may worsen these conditions. Some patients taking amantadine have attempted suicide or had suicidal ideation.

If patient has a history of heart failure or peripheral edema, monitor for weight gain and edema because drug may cause redistribution of body fluid.

Amantadine may increase seizure activity in patients with a history of seizures.
WARNING Monitor patient for evidence of neuroleptic malignant syndrome during dosage reduction or discontinuation of therapy. These include fever, hypertension or hypotension, involuntary motor activity, mental changes, muscle rigidity, tachycardia, and tachypnea. Be prepared to provide supportive treatment and additional drug therapy, as prescribed.

Be aware that patients receiving more than 200 mg daily are more likely to experience adverse or toxic reactions.

Monitor patient for decreased drug effectiveness over time. If therapeutic response declines, expect to increase dosage or discontinue drug temporarily, as ordered.

Assess patient regularly for skin changes because melanoma risk is higher in those with Parkinson’s disease. It isn’t clear whether the risk is increased by the disease or by its treatment.

PATIENT SAFTY

Instruct patient to take amantadine exactly as prescribed and not to stop abruptly. Advise patient to notify prescriber if drug becomes less effective.

Tell patient to notify prescriber if influenza symptoms don’t improve after 2 to 3 days.
WARNING Advise patient or family member to notify prescriber immediately if patient reveals thoughts of suicide.

Encourage patient to avoid consuming alcohol during amantadine therapy because alcohol may increase the risk of confusion, dizziness, light-headedness, or orthostatic hypotension.

Advise patient to avoid driving and other activities that require a high level of alertness until he knows how the drug affects him because it may cause blurred vision and mental impairment.

Advise patient to change positions slowly to minimize effects of orthostatic hypotension.

Tell patient to use ice chips or sugarless candy or gum to relieve dry mouth.

Caution patient to resume physical activities gradually as signs and symptoms improve.

Urge patient to have regular skin examinations by a dermatologist or other qualified health professional.

Instruct patient to notify prescriber about intense urges, such as for gambling or sex, because dosage may need to be reduced or drug discontinued.

Category

Chemical class: Synthetic quaternary ammonium compound
Therapeutic class:Antimyasthenic,cholinergic

Pregnancy category: C

Indications

To improve muscle strength in patients with myasthenia gravis in whom pyridostigmine or neostigmine are contraindicated Adults and adolescents. Initial: 5 mg t.i.d. or q.i.d., increased at 1to 2-day intervals to optimum dosage based on patient response. Usual: Highly individualized but usually 5 to 50 mg t.i.d. or q.i.d. Children. Initial: 0.3 mg/kg or 10 mg/m2 daily in divided doses t.i.d. or q.i.d. Maintenance: Up to 1.5 mg/kg or 50 mg/m2 daily in divided doses t.i.d. or q.i.d. Route Onset Peak Duration P.O. 20–30 min Unknown 3–8 hr

Mechanism of Action

Attaches to acetylcholinesterase and blocks its breakdown. This action prolongs and exaggerates acetylcholine’s effects, producing cholinergic responses, such as miosis, increased intestinal and skeletal muscle tone, bronchoconstriction, bradycardia, and increased salivary and sweat gland secretion.

Contraindications

Hypersensitivity to ambenonium, its components, or anticholinesterases; mechanical intestinal or urinary tract obstruction

Interactions

anesthetics, antiarrhythmics, corticosteroids, magnesium, methocarbamol: Decreased effects of ambenonium aminoglycosides, anticholinesterase muscle stimulants, depolarizing muscle relaxants, ganglionic blockers, mecamylamine: Increased effects of ambenonium

Side Efect

CNS: Dizziness, drowsiness, headache, loss of consciousness, seizures, syncope
CV: AV block, bradycardia, decreased cardiac output, hypotension
EENT: Dysphonia, increased salivation, laryngospasm
GI: Abdominal cramps, dysphagia, flatulence, increased gastric and intestinal secretions, increased peristalsis, mild diarrhea, nausea, vomiting
GU: Incontinence, urinary frequency or urgency
MS: Arthralgia, dysarthria, fasciculations, muscle spasms, muscle weakness
RESP: Bronchoconstriction, bronchospasm, dyspnea, increased tracheobronchial secretions, lung congestion, respiratory arrest or depression, respiratory muscle paralysis
SKIN: Diaphoresis, flushing, rash, urticaria

Cautions

Increase dosage gradually as prescribed to avoid ambenonium buildup and overdose.

When increasing dosage to optimum level, note when no further increase in muscle strength is observed. Then expect to reduce dosage to previous effective level and to use this as maintenance dosage.

Expect prescriber to order ephedrine (25 mg per ambenonium dose) or potassium chloride (1 to 2 g per ambenonium dose) to further improve muscle strength.
WARNING Drug has a narrow margin between effectiveness and overdose. If patient receives more than 200 mg daily, watch closely for overdose (cholinergic crisis), such as abdominal cramps, diarrhea, nausea, vomiting, increased salivation, diaphoresis, difficulty swallowing, blurred vision, miosis, hypertension, fasciculations, and voluntary muscle paralysis.

Assess neuromuscular status to detect progressive or recurrent muscle weakness during long-term ambenonium therapy.

If patient develops drug resistance in longterm therapy, expect to restore responsiveness by decreasing dosage or briefly stopping drug with close supervision.

PATIENT SAFTY

Instruct patient to swallow tablet with liquid or food to minimize GI irritation.

Advise patient to consult prescriber before discontinuing drug—even if symptoms diminish or disappear.

Category

Chemical class: Autocrine and paracrine peptide
Therapeutic class: Endothelin receptor antagonist

Pregnancy category: X

Indications

To treat pulmonary arterial hypertension, improve exercise capacity, and delay worsening in patients with World Health Organization (WHO) class II or III symptoms
Adults. Initial: 5 mg once daily, increased to 10 mg once daily as needed and tolerated. Route Onset Peak Duration P.O. Unknown 2 hr Unknown

Mechanism of Action

Blocks the action of endothelin-1 (ET-1), a potent autocrine and paracrine peptide in vascular smooth muscle and endothelium of lung tissue. ET-1 levels increase in pulmonary arterial hypertension, and ET-1 may affect its development and progression. Ambrisentan blocks an ET-1 receptor subtype, ETA, that causes vasoconstriction and cell proliferation, decreasing pulmonary artery pressure and cell proliferation and possibly delaying disease progression.

Contraindications

Hypersensitivity to ambrisentan or its components, pregnancy, breast-feeding, moderate to severe hepatic disease

Interactions

cyclosporine A: Possibly increased exposure to ambrisentan strong CYP3A inhibitors (such as ketoconazole) and CYP2C19 inhibitors (such as omeprazole): Possibly increased plasma ambrisentan level and increased risk of toxicity grapefruit juice: Possibly increased blood ambrisentan level

Side Efect

CNS: Headache
CV: Heart failure, palpitations, peripheral edema
EENT: Nasal congestion, nasopharyngitis, sinusitis
GI: Abdominal pain, constipation, elevated liver enzymes
HEME: Anemia
RESP: Dyspnea
SKIN: Flushing
Other: Angioedema

Cautions

Ambrisentan isn’t recommended for patients with moderate to severe hepatic impairment. Use it cautiously in patients with mild hepatic impairment.

Ambrisentan is available only through a restricted distribution program. Patients must be enrolled, meet all conditions of the program, and be re-enrolled annually.

Before giving ambrisentan for the first time, make sure patient understands its risks, has signed the agreement form, and knows that he’ll need to be re-enrolled after 6 months of therapy and then yearly.

If patient is a woman of childbearing age, obtain a negative pregnancy test before giving ambrisentan and then monthly during therapy. A positive result requires immediately stopping drug because of the risk of serious birth defects.

Obtain liver enzyme levels, as ordered, before starting ambrisentan therapy and monthly during therapy because drug may significantly increase liver aminotransferase (ALT and AST) levels. If liver enzymes are more than three times the upper limit of normal. expect to not start ambrisentan. If they’re somewhat elevated, expect to monitor bilirubin before and monthly during therapy. If liver enzymes become elevated during therapy and evidence of hepatic dysfunction (abdominal pain, fever, jaundice, nausea, vomiting, unusual lethargy or fatigue) develops or patient’s bilirubin level exceeds twice the upper limit of normal, notify prescriber and expect to stop ambrisentan therapy.

Monitor patient’s hemoglobin level before starting ambrisentan, again after 1 month of therapy, and periodically thereafter. If level declines significantly, notify prescriber and expect to discontinue drug.

Assess patient closely for peripheral edema, especially if elderly. If edema becomes pronounced, notify prescriber. Further evaluation will reveal whether it results from ambrisentan or another condition, such as heart failure.

If patient takes ambrisentan for longer than 12 months, watch for hepatic cirrhosis (abdominal pain, fever, jaundice, nausea, vomiting, or unusual lethargy or fatigue). A similar drug, bosentan, rarely has caused unexplained hepatic cirrhosis after being taken longer than 12 months.

PATIENT SAFTY

Caution patient not to split, crush, or chew ambrisentan tablets.

Instruct female patient of childbearing age to use two reliable forms of birth control during therapy unless she has had a tubal ligation or a Copper T 380A or LNg 20 intrauterine device inserted. Explain that she’ll need monthly pregnancy test.

Inform male patient that sperm counts have declined in some men taking similar to ambrisentan, affecting their ability to father children. If this concerns him, suggest that he consult prescriber.

Stress the need for follow-up visits and tests, such as hemoglobin checks.

Advise patient to promptly report any signs of liver dysfunction to the prescriber.

Instruct patient to notify prescriber about fluid retention.

Category

Chemical class: Aminoglycoside
Therapeutic class: Antibiotic

Pregnancy category: D

Indications

To treat serious gram-negative bacterial infections (including septicemia; neonatal sepsis; respiratory tract, bone, joint, CNS, skin, soft-tissue, intra-abdominal, burn, and postoperative infections; and serious, complicated, and recurrent UTI) caused by Acinetobacter, Enterobacter, Escherichia coli, Klebsiella, Proteus, Providencia, Pseudomonas, and Serratia; and staphylococcal infections when penicillin is contraindicated
IV:,
I.M.INJECTION Adults and children.15 mg/kg daily in equal doses at equally spaced intervals (7.5 mg/kg every 12 hr or 5 mg/kg every 8 hr) for 7 to 10 days. Maximum: 1,500 mg daily.
DOSAGE ADJUSTMENT For patients with impaired renal function, loading dose of 7.5 mg/kg daily; then maintenance dosage based on creatinine clearance and serum creatinine level and given every 12 hr. For morbidly obese patients, dosage not to exceed 1.5 g daily. Neonates. Loading dose: 10 mg/kg. Maintenance: 7.5 mg/kg every 12 hr for 7 to 10 days. To treat uncomplicated UTI
IV:,
I.M.INJECTION
Adults.250 mg b.i.d. for 7 to 10 days. Route Onset Peak Duration I.V. Immediate Unknown Unknown I.M. Rapid Unknown Unknown

Mechanism of Action

Binds to negatively charged sites on bacteria’s outer cell membrane, disrupting cell integrity. Also binds to bacterial ribosomal subunits and inhibits protein synthesis. Both actions lead to cell death. Incompatibilties Don’t mix or infuse amikacin with other .

Contraindications

Hypersensitivity to amikacin or other aminoglycosides

Interactions

cephalosporins, enflurane, methoxyflurane, vancomycin: Increased nephrotoxic effects general anesthetics: Increased risk of neuromuscular blockade loop diuretics: Increased risk of ototoxicity neuromuscular blockers: Possibly increased neuromuscular blockade and prolonged respiratory depression penicillins: Possibly inactivation of or synergistic effects with amikacin

Side Efect

CNS: Drowsiness, headache, loss of balance, neuromuscular blockade, tremor, vertigo
EENT: Hearing loss, ototoxicity, tinnitus amikacin sulfate 60
GI: Nausea, vomiting
GU: Azotemia, dysuria, nephrotoxicity, oliguria or polyuria, proteinuria
MS: Acute muscle paralysis; arthralgia; muscle fatigue, spasms, and weakness
RESP: Apnea
Other: Hyperkalemia

Cautions

Expect to obtain results of culture and sensitivity testing before therapy begins.

Prepare amikacin I.V. solution by adding contents of 500-mg vial to 100 to 200 ml of sterile diluent. Then infuse drug over 30 to 60 minutes.

Give I.M. injection in large muscle mass.

Watch for signs of ototoxicity, such as tinnitus and vertigo, especially during highdosage or prolonged amikacin therapy.
WARNING Because amikacin may produce nephrotoxic effects, assess renal function before and daily during therapy, as ordered. To minimize renal tubule irritation, maintain hydration during therapy.

Be aware that amikacin may exacerbate muscle weakness in such conditions as myasthenia gravis and Parkinson’s disease.

Measure serum amikacin concentrations as ordered, usually 30 to 90 minutes after injection (for peak concentration) and just before administering next dose (for trough concentration).

PATIENT SAFTY

Tell patient that daily laboratory tests are necessary during treatment.

Instruct patient to report ringing in ears, hearing changes, headache, nausea, vomiting, and changes in urination.

Category

Chemical class: Pyrazine-carbonylguanidine
Therapeutic class: Potassium-sparing diuretic

Pregnancy category: B

Indications

As adjunct to thiazide or loop diuretic in patient with heart failure or hypertension to correct diuretic-induced hypokalemia or to prevent diuretic-induced hypokalemia that increases the risk of arrhythmias or other complications
Adults. 5 to 10 mg daily as single dose; if hypokalemia persists, increased to 15 mg daily and then 20 mg daily. Route Onset Peak Duration P.O. 2 hr 6–10 hr 24 hr

Mechanism of Action

Inhibits sodium reabsorption in distal convoluted tubules and cortical collecting ducts, causing sodium and water loss and enhancing potassium retention.

Contraindications

Hypersensitivity to amiloride; impaired renal function; serum potassium level above 5.5 mEq/L; therapy with another potassiumsparing diuretic, such as spironolactone or triamterene, or a potassium supplement

Interactions

angiotensin II receptor antagonists, captopril, enalapril, lisinopril, potassium products, spironolactone: Increased risk of hyperkalemia digoxin: Decreased effectiveness of digoxin lithium: Reduced renal clearance of lithium and increased risk of lithium toxicity
NSAIDs: Reduced diuretic effect of amiloride sympathomimetics: Possibly reduced antihypertensive effects of amiloride high-potassium food: Increased risk of hyperkalemia

Side Efect

CNS: Confusion, depression, dizziness, drowsiness, encephalopathy, fatigue, headache, insomnia, nervousness, paresthesia, somnolence, tremor, vertigo
CV: Angina, arrhythmias, orthostatic hypotension, palpitations
EENT: Dry mouth, increased intraocular pressure, nasal congestion, tinnitus, vision disturbances
GI: Abdominal pain or fullness, anorexia, appetite changes, constipation, diarrhea, GI bleeding, heartburn, indigestion, nausea, thirst, vomiting
GU: Bladder spasms, dysuria, impotence, loss of libido, polyuria
HEME: Aplastic anemia, neutropenia
MS: Arthralgia, muscle spasms or weakness
RESP: Cough, dyspnea
SKIN: Alopecia, jaundice, pruritus, rash
Other: Dehydration, hyperchloremia, hyperkalemia, hypernatremia, metabolic acidosis

Cautions

Administer amiloride with food to reduce GI upset and early in the day to minimize sleep interference from polyuria.

Monitor renal function test results, fluid intake and output, and weight. Also monitor serum potassium level to detect hyperkalemia.
WARNING Don’t administer amiloride with other potassium-sparing diuretics.

PATIENT SAFTY

Warn patient to avoid high-potassium food and salt substitutes that contain potassium.

Advise patient to consult prescriber before taking other , including OTC remedies, especially sympathomimetics.

Tell patient to report dizziness, trembling, numbness, and muscle weakness or spasms.

Advise patient to increase fluid and fiber intake to prevent constipation.

Warn patient to expect reversible hair loss and impotence.

Category

Chemical class: Aminohexanoic acid
Therapeutic class: Antifibrinolytic, antihemorrhagic

Pregnancy category: C

Indications

To treat excessive bleeding caused by fibrinolysis SYRUP,
Adults. Initial: 5 g in first hour, followed by 1 to 1.25 g/hr to sustain drug plasma level of 0.13 mg/ml. Maximum: 30 g daily.
I.V.INJECTION
Adults.4 to 5 g in 250 ml of diluent over 1 hr followed by continuous infusion of 1 g/hr in 50 ml of diluent. Continue for 8 hr or until bleeding stops. Route Onset Peak Duration P.O. Rapid Unknown Unknown I.V. Immediate Unknown Under 3 hr

Mechanism of Action

Inhibits breakdown of blood clots by interfering with plasminogen activator substances and producing antiplasmin activity.

Contraindications

Hypersensitivity to aminocaproic acid; signs of active intravascular clotting, as in disseminated intravascular coagulation; upper urinary tract bleeding

Interactions

activated prothrombin, prothrombin complex concentrates: Increased risk of thrombosis estrogens, oral contraceptives: Increased risk of hypercoagulation

Side Efect

CNS: Delirium, dizziness, hallucinations, headache, malaise, stroke, weakness
CV: Bradycardia, cardiomyopathy, elevated serum CK level, hypotension, ischemia, thrombophlebitis
EENT: Nasal congestion, tinnitus
GI: Abdominal cramps and pain, diarrhea, elevated AST level, nausea, vomiting
GU: Elevated BUN level, intrarenal obstruction, renal failure
HEME: Agranulocytosis, leukopenia, thrombocytopenia
MS: Myopathy
RESP: Dyspnea, pulmonary embolism
SKIN: Pruritus, rash
Other: Elevated serum aldolase and potassium levels

Cautions

Be aware that patients on oral therapy may need up to 10 tablets during the first hour of treatment and tablets around the clock during continued treatment.

Mix aminocaproic acid solution with sterile water for injection, normal saline solution, D5W, or Ringer’s solution.
WARNING Avoid rapid I.V. delivery because aminocaproic acid 62 it increases risk of hypotension and bradycardia.

Monitor neurologic status for druginduced changes. Note that increased clotting may lead to stroke.

PATIENT SAFTY

Tell patient that he’ll be closely monitored during I.V. therapy and will have blood drawn for laboratory tests before, during, and after treatment.

Advise patient who takes aminocaproic acid at home to report

Side Efect

, take drug exactly as prescribed, and keep follow-up appointments with prescriber.

Category

Chemical class: Hormone
Therapeutic class: Adrenal steroid inhibitor

Pregnancy category: D

Indications

To suppress adrenal function in patients with Cushing’s syndrome who are waiting for surgery or for whom other treatment can’t be used
Adults.Initial: 250 mg every 6 hr. Increased as needed by 250 mg daily every 1 to 2 wk. Maximum: 2,000 mg daily. Route Onset Peak Duration P.O. 3–5 days Unknown 72 hr

Mechanism of Action

Inhibits the conversion of cholesterol to delta-5-pregnenolone, which is needed to produce certain hormones, including adrenal glucocorticoids, mineralocorticoids, estrogens, and androgens.

Contraindications

Hypersensitivity to aminoglutethimide or glutethimide

Interactions

antidiabetics, dexamethasone, digoxin, medroxyprogesterone, synthetic glucocorticoids, theophylline, warfarin and other oral anticoagulants: Decreased effects of these

Side Efect

CNS: Dizziness, drowsiness, fever, headache
CV: Hypotension, orthostatic hypotension, tachycardia
ENDO: Adrenal insufficiency, hypothyroidism, masculinization
GI: Anorexia, nausea
SKIN: Hair growth, morbiliform rash, pruritus, urticaria

Cautions

Expect to reduce aminoglutethimide dosage or discontinue treatment if extreme drowsiness, severe rash, or excessively low cortisol level occurs.
WARNING Monitor for signs of hypothyroidism, including lethargy, dry skin, and slow pulse. If prescribed, administer thyroid hormone supplement.

Monitor blood pressure for orthostatic or persistent hypotension.

PATIENT SAFTY

Teach patient to recognize orthostatic hypotension (dizziness, weakness when moving from sitting to standing position) and to minimize it (as by rising slowly from a supine to an upright position).

Tell patient to report dizziness, appetite loss, nausea, headache, or severe drowsiness. Warn him to avoid driving if drowsy.

Instruct patient to take a missed dose as soon as remembered and to evenly space out the day’s remaining doses.

Advise patient that rash, sometimes accompanied by fever, may appear on day 10 of treatment and should subside by day 15 or 16. Tell him to report severe rash or one that doesn’t disappear.

Category

Chemical class: Xanthine
Therapeutic class: Bronchodilator

Pregnancy category: C

Indications

To relieve acute bronchospasm
IV: Adults and children not currently receiving theophylline products.Initial: 6 mg/kg (equal to 4.7 mg/kg anhydrous theophylline), not to exceed 25 mg/min. Maintenance: For adults (nonsmokers), 0.7 mg/kg/hr for first 12 hr, then 0.5 mg/kg/ hr. For children ages 9 to 16, 1 mg/kg/hr for first 12 hr, then 0.8 mg/kg/hr. For children ages 6 months to 9 years and young adult smokers, 1.2 mg/kg/hr for first 12 hr, then 1 mg/kg/hr. Adults and children currently receiving theophylline products. Initial: If possible, determine the time, amount, administration route, and form of last dose. Loading dose is based on the principle that each 0.63 mg/kg (0.5 mg/kg anhydrous theophylline) given raises serum theophylline level by 1 mcg/ml. Defer loading dose if serum theophylline level can be readily obtained. If this isn’t possible and patient has no obvious signs of theophylline toxicity, prescriber may order 3.1 mg/kg (2.5 mg/ kg anhydrous theophylline), which may increase serum theophylline level by about 5 mcg/ml. Maintenance: For adults (nonsmokers), 0.7 mg/kg/hr for first 12 hr, then 0.5 mg/kg/hr. For children ages 9 to 16, 1 mg/kg/hr for first 12 hr, then 0.8 mg/kg/hr. For children ages 6 months to 9 years and young adult smokers, 1.2 mg/kg/hr for first 12 hr, then 1 mg/kg/hr.
DOSAGE ADJUSTMENT For elderly patients and those with cor pulmonale, dosage reduced to 0.6 mg/kg for 12 hr, then 0.3 mg/kg. For patients with heart failure and hepatic disease, dosage reduced to 0.5 mg/kg for 12 hr, then 0.1 to 0.2 mg/kg. To prevent or treat reversible bronchospasm from asthma, chronic bronchitis, and emphysema and to maintain patent airways ,ORALLIQUID,,SUPPOSITORIES Adults and children.Initial (rapidly absorbed forms): 16 mg/kg daily or 400 mg daily (whichever is less) in divided doses every 6 to 8 hr. Maintenance: Daily dosage increased in increments of 25% every 3 days, as tolerated, until response achieved or maximum dose reached. When maximum dose is reached, dosage adjusted according to peak serum theophylline level. Initial ( forms): 12 mg/kg daily or 400 mg daily (whichever is less) in divided doses every 8 to 12 hr. Maintenance: Daily dosage increased in increments of 2 to 3 mg/kg every 3 days. When maximum dose is reached, dosage adjusted according to peak serum theophylline level. Route Onset Peak Duration P.O. ()Unknown Unknown 8–12 hr P.O. (tab) Unknown Unknown 6–8 hr I.V. Immediate Unknown 4–8 hr

Mechanism of Action

Inhibits phosphodiesterase enzymes, causing bronchodilation. Normally, these enzymes inactivate cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), which are responsible for bronchial smooth-muscle relaxation. Other mechanisms of action may include translocation of calcium, prostaglandin antagonism, stimulation of catecholamines, inhibition of cGMP metabolism, and adenosine receptor antagonism.

Incompatibilities

Don’t add other to prepared bag or bottle of aminophylline. Don’t mix aminophylline in same syringe with doxapram. Also avoid administering amiodarone, ciprofloxacin, diltiazem, dobutamine, hydralazine, or ondansetron into the Y-port of a continuous infusion of aminophylline.

Contraindications

Active peptic ulcer disease, hypersensitivity to aminophylline, rectal or lower intestine irritation or infection (suppository form), underlying seizure disorder

Interactions

activated charcoal, aminoglutethimide, barbiturates, ketoconazole, rifampin, sulfinpyrazone, sympathomimetics: Decreased serum theophylline level allopurinol, calcium channel blockers, cimetidine, corticosteroids, disulfiram, ephedrine, influenza virus vaccine, interferon, macrolides, mexiletine, nonselective beta blockers, oral contraceptives, quinolones, thiabendazole: Increased serum theophylline level benzodiazepines: Antagonized sedative effects of benzodiazepines beta agonists: Increased effects of aminophylline and beta agonist carbamazepine, isoniazid, loop diuretics: Altered serum theophylline level halothane: Increased risk of cardiotoxicity hydantoins: Decreased hydantoin level ketamine: Increased risk of seizures lithium: Decreased serum lithium level nondepolarizing muscle relaxants: Reversed neuromuscular blockade propofol: Antagonized sedative effects of propofol tetracyclines: Enhanced adverse effects of theophylline all : Altered bioavailability and absorption of form, leading to toxicity high-carbohydrate, low-protein diet: Decreased theophylline elimination and prolonged aminophylline half-life low-carbohydrate, high-protein diet; charbroiled beef: Increased theophylline elimination and shortened aminophylline half-life alcohol abuse: Increased aminophylline effects smoking (1 or more packs daily): Decreased effects of aminophylline

Side Efect

CNS: Dizziness, fever, headache, insomnia, irritability, restlessness, seizures
CV: Arrhythmias (including sinus tachycardia and life-threatening ventricular arrhythmias), hypotension, palpitations
EENT: Bitter aftertaste
ENDO: Hyperglycemia, syndrome of inappropriate ADH secretion
GI: Anorexia, diarrhea, epigastric pain, heavy feeling in stomach, hematemesis, indigestion, nausea, rectal bleeding or irritation (suppositories), vomiting
GU: Diuresis, proteinuria, urine retention in men with prostate enlargement
MS: Muscle twitching
RESP: Respiratory arrest, tachypnea
SKIN: Alopecia, exfoliative dermatitis, flushing, rash, urticaria

Cautions

WARNING Because aminophylline has a narrow therapeutic window (10 to 20 mcg/ ml), closely monitor serum theophylline level and watch for evidence of toxicity (tachycardia, tachypnea, nausea, vomiting, restlessness, seizures). Keep in mind that acetaminophen, furosemide, phenylbutazone, probenecid, theobromine, coffee, tea, soft drinks, and chocolate can alter serum theophylline result.

To determine peak serum theophylline level, draw blood sample 15 to 30 minutes after administering I.V. loading dose.

Give immediate-release and liquid forms with food to reduce GI upset. Give form 1 hour before or 2 hours after meals because food can alter drug absorption.

PATIENT SAFTY

Advise patient to avoid excessive caffeine (in coffee, tea, soft drinks, and chocolate); it can falsely elevate theophylline level.

Explain that blood tests may be needed to monitor drug’s therapeutic effect.

Category

Chemical class: Para-aminobenzoic acid analogue
Therapeutic class: Antitubercular

Pregnancy category: C

Indications

To treat tuberculosis as adjunct to isoniazid, streptomycin, or both and in patients with multidrug-resistant tuberculosis or when therapy with rifampin and isoniazid isn’t possible because of resistance or intolerance
Adults. 14 to 16 g daily in 2 or 3 divided doses. Children. 275 to 420 mg/kg daily in 3 or 4 divided doses.

Mechanism of Action

Inhibits incorporation of para-aminobenzoic acid into folic acid and prevents synthesis of folic acid, a compound needed for bacterial growth. Aminosalicylate sodium is bacteriostatic against Mycobacterium tuberculosis, and it delays bacterial resistance to streptomycin and isoniazid.

Contraindications

Hypersensitivity to aminosalicylate sodium, severe renal disease

Interactions

digoxin: Decreased serum digoxin level probenecid: Increased serum aminosalicylate level
rifampin: Decreased serum rifampin level

Side Efect

CNS: Encephalopathy, fever
CV: Vasculitis
ENDO: Goiter with or without myxedema
GI: Abdominal pain, diarrhea, hepatitis, nausea, vomiting
HEME: Agranulocytosis, hemolytic anemia, leukopenia, thrombocytopenia
SKIN: Jaundice, various types of eruptions
Other: Infectious mononucleosis-like syndrome, Loeffler’s syndrome (anorexia, breathlessness, fever, and weight loss)

Cautions

Administer aminosalicylate with food to reduce GI upset.
WARNING Protect drug from water, heat, and sunlight to prevent rapid deterioration. Don’t give tablets with brown or purple discoloration—a sign of deterioration.

PATIENT SAFTY

Teach patient to discard aminosalicylate that appears brown or purple.

Instruct patient to take drug with food.

Category

Chemical class: Iodinated benzofuran derivative
Therapeutic class: Class III antiarrhythmic

Pregnancy category: D

Indications

To treat life-threatening, recurrent ventricular fibrillation and hemodynamically unstable ventricular tachycardia when these arrhythmias don’t respond to other or when patient can’t tolerate other
Adults.Loading: 800 to 1,600 mg daily in divided doses for 1 to 3 wk. Maintenance: 600 to 800 mg daily in divided doses for 1 mo; then if cardiac rhythm is stable, 400 mg daily in 1 or 2 doses. Use lowest possible dose.
IV:
Adults.Loading: 150 mg over 10 min (15 mg/ min) followed by 360 mg infused over 6 hr (1 mg/min). Maintenance: 540 mg infused over 18 hr (0.5 mg/min); then after the first 24 hr, 720 mg infused over 24 hr (0.5 mg/ min), continued up to 2 to 3 wk, as needed. Rate may be increased in first 24 hr, if needed, but initial infusion rate shouldn’t exceed 30 mg/min. Change to oral form as soon as possible. To treat breakthrough episodes of ventricular fibrillation or hemodynamically unstable ventricular tachycardia
IV:(NEXTERONE)
Adults.150 mg mixed in 100 ml D5W and infused over 10 min (15 mg/min). Route Onset Peak Duration P.O. 2 days– 1–5 mo Weeks– 3 wk months I.V. Hours– 1–3 wk Weeks– 3 days months

Mechanism of Action

Acts on cardiac cell membranes, prolonging repolarization and the refractory period and raising ventricular fibrillation threshold. Drug relaxes vascular smooth muscles, mainly in coronary circulation, and improves myocardial blood flow. It relaxes peripheral vascular smooth muscles, decreasing peripheral vascular resistance and myocardial oxygen consumption.

Incompatibilities

Amiodarone is incompatible with heparin. To prevent precipitation, don’t add amiodarone admixed with D5W to aminophylline 4 mg/ml, cefamandole nafate, cefazolin sodium, or mezlocillin sodium, and don’t mix amiodarone 3 mg/ml with sodium bicarbonate. Also, don’t use evacuated glass containers for admixing because precipitation may occur.

Contraindications

Bradycardia that causes syncope (unless pacemaker present), cardiogenic shock, hypersensitivity to amiodarone or its components, hypokalemia, hypomagnesemia, amiodarone hydrochloride 66 SA node dysfunction, secondand thirddegree AV block (unless pacemaker present)

Interactions

anticoagulants: Increased anticoagulant response and possibly serious bleeding azole antifungals, fluoroquinolones, macrolide antibiotics: Increased risk of prolonged QT interval and life-threatening arrhythmias
beta blockers: Increased serum levels of beta blockers with increased risk of AV block, hypotension, and bradycardia calcium channel blockers: Increased serum levels of these and increased risk of AV block, bradycardia, and hypotension cholestyramine, phenytoin, rifampin, St. John’s wort: Decreased amiodarone level
cimetidine: Increased amiodarone level clopidogrel: Increased risk of ineffective inhibition of platelet aggregation cyclosporine: Increased cyclosporine level dextromethorphan, methotrexate,
phenytoin: Increased serum levels of these and increased risk of toxicity if amiodarone is taken orally for more than 2 weeks digoxin: Increased serum digoxin level and risk of digitalis toxicity diltiazem, propranolol, verapamil: Increased risk of hemodynamic and electrophysiologic abnormalities disopyramide: Increased serum disopyramide level with QT prolongation and increased risk of arrhythmias fentanyl: Increased serum fentanyl level with increased risk of bradycardia, decreased cardiac output, and hypotension flecainide: Increased serum flecainide level HMG-CoA reductase inhibitors such as atorvastatin and simvastatin: Increased risk of myopathy and rhabdomyolysis hydantoins: Increased serum hydantoin level with long-term use and reduced serum amiodarone level lidocaine: Increased serum lidocaine level and risk of seizures and bradycardia loratadine, trazodone: Increased risk of QTinterval prolongation and torsades de pointes potassiumand magnesium-depleting : Increased risk of hypokalemia and hypomagnesemia procainamide: Increased serum procainamide or N-acetylprocainamide level
quinidine: Increased serum quinidine level with risk of life-threatening arrhythmias ritonavir: Increased serum amiodarone level with increased risk of cardiotoxicity
theophylline: Increased serum theophylline level; increased risk of theophylline toxicity
warfarin: Increased PT and risk of bleeding grapefruit juice: Increased amiodarone level

Side Efect

CNS: Abnormal gait, ataxia, confusion, delirium, demyelinating polyneuropathy, disorientation, dizziness, fatigue, fever, hallucinations, headache, insomnia, involuntary motor activity, lack of coordination, malaise, paresthesia, parkinsonian symptoms, peripheral neuropathy, pseudotumor cerebri, sleep disturbances, tremor
CV: Arrhythmias (including bradycardia, electromechanical dissociation, torsades de pointes, and ventricular tachycardia or fibrillation), cardiac arrest, cardiogenic shock, edema, heart failure, hypotension, vasculitis
EENT: Abnormal salivation, abnormal taste and smell, blurred vision, corneal microdeposits, dry eyes, halo vision, lens opacities, macular degeneration, optic neuritis, optic neuropathy, papilledema, permanent blindness, photophobia, scotoma
ENDO: Hyperthyroidism, hypothyroidism, syndrome of inappropriate ADH secretion, thyroid cancer
GI: Abdominal pain, anorexia, cirrhosis, constipation, diarrhea, elevated liver function test results, hepatitis, nausea, pancreatitis, vomiting
GU: Acute renal failure, decreased libido, epididymitis, impotence
HEME: Agranulocytosis, aplastic or hemolytic anemia, coagulation abnormalities, neutropenia, pancytopenia, spontaneous bruising, thrombocytopenia
MS: Muscle weakness, myopathy, rhabdomyolysis
RESP: Acute respiratory distress syndrome; bronchospasm; eosinophilic pneumonia; infiltrates that lead to dyspnea, cough, hemoptysis, hypoxia, pulmonary fibrosis, pulmonary alveolar hemorrhage, pulmonary interstitial pneumonitis, crackles, and wheezing; pleural effusion; pleuritis; pneumonia; respiratory arrest or failure
SKIN: Alopecia, bluish gray pigmentation, eczema, erythema multiforme, exfoliative dermatitis, flushing, photosensitivity, pruritus, rash, skin cancer, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylactic shock, angioedema

Cautions

If patient has an implantable cardiac device, have it checked, as ordered, at the start of and during amiodarone therapy because drug may affect pacing or defibrillating thresholds.

Parenteral amiodarone may be diluted in D5W or normal saline solution and given in polyvinvyl chloride (PVC), polyolefin, or glass containers.

Use an in-line filter during I.V. administration of amiodarone. Also use a central venous catheter whenever possible. A central venous catheter is required when infusion rate exceeds 2 mg/ml because drug may cause peripheral vein phlebitis at higher rates. Cordarone I.V. must be given by volumetric infusion pump.

Monitor amiodarone I.V. infusion closely because loading doses at higher concentrations and rates may cause hepatocellular necrosis, acute renal failure, and death.

Although maintenance therapy usually is needed for only up to 96 hours, infusion of up to 0.5 mg/minute may be continued for 2 to 3 weeks regardless of patient’s age, renal function, or left ventricular function.
WARNING Amiodarone may cause or worsen pulmonary disorders that may develop days to weeks after therapy and progress to respiratory failure or even death. Expect to obtain chext x-ray and pulmonary function tests before therapy starts and then chest x-ray and follow-up exams every 3 to 6 months during therapy.

Monitor vital signs and oxygen level often during and after giving amiodarone. Keep emergency equipment and nearby.
WARNING Monitor continuous ECG; check for increased PR and QRS intervals, arrhythmias, and heart rate below 60 beats/min because amiodarone toxicity may cause or worsen arrhythmias.

Monitor serum amiodarone level, which normally ranges from 1.0 to 2.5 mcg/ml.

Assess liver enzyme and thyroid hormone levels; drug inhibits conversion of T4to T3 and may cause drug-induced hyperthyroidism, thyrotoxicosis, and new or worsened arrhythmias. If new signs of arrhythmia occur, notify prescriber at once.

PATIENT SAFTY

Explain that patient will need frequent monitoring and laboratory tests during treatment.

Advise patient to report swollen hands and feet, wheezing, dyspnea, cough, nausea, vomiting, dark urine, fatigue, yellow skin or sclerae, stomach pain, light-headedness, fainting, or a rapid, slow, pounding, or irregular heartbeat.

Instruct patient to report abnormal bleeding or bruising.

Advise patient to avoid corneal refractive laser surgery while taking drug.

Category

Chemical class: Tertiary amine
Therapeutic class: Tricyclic antidepressant

Pregnancy category: D

Indications

To relieve depression, especially when accompanied by anxiety and insomnia Adults and children over age 12. Outpatient: 75 mg daily in divided doses, increased to 150 mg daily, if needed. Inpatient: 100 mg daily, gradually increased to 300 mg daily, if needed. Maintenance: 40 to 100 mg daily at bedtime.
DOSAGE ADJUSTMENT Maintenance dosage reduced to 10 mg t.i.d. plus 20 mg at bedtime for adolescent and elderly patients. Route Onset Peak Duration P.O. 14–21 Unknown Unknown days

Contraindications

Acute recovery phase after MI, hypersensitivity to amitriptyline, MAO inhibitor therapy within 14 days

Interactions

anticholinergics, epinephrine, norepinephamitriptyline hydrochloride : Increased effects of these barbiturates: Decreased amitriptyline level carbamazepine: Decreased serum amitriptyline level and increased serum carbamazepine level, which increases therapeutic and toxic effects of carbamazepine cimetidine, disulfiram, fluoxetine, fluvoxamine, haloperidol, H2-receptor antagonists, methylphenidate, oral contraceptives, paroxetine, phenothiazines, sertraline: Increased serum amitriptyline level cisapride: Possibly prolonged QT interval and increased risk of arrhythmias clonidine, guanethidine, and other antihypertensives: Decreased antihypertensive effects dicumarol: Increased anticoagulant effect levodopa: Decreased levodopa absorption; sympathetic hyperactivity, sinus tachycardia, hypertension, agitation
MAO inhibitors: Possibly seizures and death thyroid replacement : Arrhythmias and increased antidepressant effects
alcohol use: Enhanced CNS depression smoking: Decreased amitriptyline effects

Side Efect

CNS: Anxiety, ataxia, coma, chills, delusions, disorientation, drowsiness, extrapyramidal reactions, fatigue, fever, headache, insomnia, nightmares, peripheral neuropathy, suicidal ideation, tremor
CV: Arrhythmias (including prolonged AV conduction, heart block, and tachycardia), cardiomyopathy, hypertension, MI, nonspecific ECG changes, orthostatic hypotension, palpitations
EENT: Abnormal taste, black tongue, blurred vision, dry mouth, increased salivation, nasal congestion, tinnitus
ENDO: Gynecomastia, increased or decreased blood glucose level, increased prolactin level, syndrome of inappropriate ADH secretion
GI: Abdominal cramps, constipation, diarrhea, flatulence, ileus, increased appetite, nausea, vomiting
GU: Impotence, libido changes, menstrual irregularities, testicular swelling, urinary hesitancy, urine retention
HEME: Agranulocytosis, bone marrow depression, eosinophilia, leukopenia, thrombocytopenia
SKIN: Alopecia, flushing, purpura
Other: Weight gain

Cautions

Because of amitriptyline’s atropine-like effects, use caution if patient has a history .Normally, when an impulse reaches adrenergic nerves, the nerves release serotonin and norepinephrine from their storage sites. Some serotonin and norepinephrine reaches receptor sites on target tissues. Most is taken back into the nerves and stored by the reuptake mechanism, as shown below on the left. Amitriptyline blocks serotonin and norepinephrine reuptake by adrenergic nerves. By doing so, it raises serotonin and norepinephrine levels at nerve synapses. This action may elevate mood and reduce depression. Nerve impulse Serotonin reuptake Serotonin Adrenergic nerve Norepinephrine reuptake Norepinephrine Receptor sites Reuptake blocked by amitriptyline

Mechanism of Action

of seizures, urine retention, or angleclosure glaucoma.
WARNING Don’t give an MAO inhibitor within 14 days of amitriptyline because of the risk of seizures and death.

Closely monitor patient with CV disorder because amitriptyline may cause arrhythmias, such as sinus tachycardia.

Watch patients closely (especially children, adolescents, and young adults), for suicidal tendencies, particularly when therapy starts and dosage changes. Depression may worsen temporarily during these times.

Monitor blood pressure for hypotension or hypertension.

Stay alert for behavior changes, such as hallucinations and decreased interest in personal appearance. Be aware that psychosis may develop in schizophrenic patients, and symptoms may increase in paranoid patients.

Abrupt withdrawal after long use may cause nausea, headache, vertigo, and nightmares.

PATIENT SAFTY

Instruct patient to take amitriptyline at bedtime to avoid daytime drowsiness.

Instruct patient to avoid using alcohol or OTC that contain alcohol during amitriptyline therapy because alcohol enhances CNS depressant effects.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes and particularly if patient is a child, teenager, or young adult.

Category

Chemical class: Dihydropyridine
Therapeutic class: Antianginal, antihypertensive

Pregnancy category: C

Indications

To control hypertension
Adults.Initial: 5 mg daily, increased gradually over 10 to 14 days, as needed. Maximum: 10 mg daily.
DOSAGE ADJUSTMENT Initially 2.5 mg daily for elderly patients or patients with impaired hepatic function. Increased gradually over 7 to 14 days based on response. To treat chronic stable angina and Prinzmetal’s (variant) angina
Adults.5 to 10 mg daily.
DOSAGE ADJUSTMENT 5 mg daily for elderly patients and those with impaired hepatic function. Route Onset Peak Duration P.O. Unknown 6–12 hr 24 hr

Mechanism of Action

Binds to dihydropyridine and nondihydropyridine cell membrane receptor sites on myocardial and vascular smooth-muscle cells and inhibits influx of extracellular calcium ions across slow calcium channels. This decreases intracellular calcium level, inhibiting smooth-muscle cell contractions and relaxing coronary and vascular smooth muscles, decreasing peripheral vascular resistance, and reducing systolic and diastolic blood pressure. Decreased peripheral vascular resistance also decreases myocardial workload, oxygen demand, and possibly angina. Also, by inhibiting coronary artery muscle cell contractions and restoring blood flow, drug may relieve Prinzmetal’s angina.

Contraindications

Hypersensitivity to amlodipine or its components

Interactions

beta blockers: Possibly excessive hypotension fentanyl: Increased risk of severe hypotension and increased fluid volume requirements during surgery

Side Efect

CNS: Anxiety, dizziness, fatigue, headache, lethargy, light-headedness, paresthesia, somnolence, syncope, tremor
CV: Arrhythmias, hypotension, palpitations, peripheral edema
EENT: Dry mouth, pharyngitis
ENDO: Hot flashes
GI: Abdominal cramps, abdominal pain, constipation, diarrhea, esophagitis, indigestion, nausea amlodipine besylate 70
GU: Decreased libido, impotence, urinary frequency
MS: Myalgia
RESP: Dyspnea
SKIN: Dermatitis, flushing, rash
Other: Weight loss

Cautions

Use amlodipine cautiously in patients with heart block, heart failure, impaired renal function, hepatic disorder, or severe aortic stenosis.

Monitor blood pressure while adjusting dosage, especially in patients with heart failure or severe aortic stenosis.

PATIENT SAFTY

Tell patient to take missed dose as soon as remembered and next dose in 24 hours.

Tell patient to immediately notify prescriber of dizziness, arm or leg swelling, difficulty breathing, hives, or rash.

Suggest taking amlodipine with food to reduce GI upset.

Advise patient to routinely have blood pressure checked for possible hypotension.

Category

Chemical class: Ammonium ion
Therapeutic class: Acidifier

Pregnancy category: C

Indications

To treat hypochloremia and metabolic alkalosis
IV:
Adults.Individualized based on serum bicarbonate level. Usual: 100 to 200 mEq added to 500 or 1,000 ml of normal saline solution, infused at 5 ml/min or less (about 3 hr for an infusion of 1,000 ml). Route Onset Peak Duration I.V. 1–3 min 3–6 hr Unknown

Mechanism of Action

Is converted to urea and hydrochloric acid in the liver. During conversion, drug breaks into ammonium and chloride ions, and hydrogen ions are released. They enter the blood and extracellular fluid, where hydrogen reacts with bicarbonate ions to form water and carbon dioxide. This process decreases bicarbonate ions and increases chloride ions in blood and extracellular fluid, which decreases blood and urine pH and corrects alkalosis.

Incompatibilities

Don’t mix I.V. ammonium chloride with codeine, levorphanol, or methadone.

Contraindications

Hypersensitivity to ammonium chloride or its components, markedly impaired renal or hepatic function, metabolic alkalosis caused by vomiting of hydrochloric acid and accompanied by sodium loss caused by sodium bicarbonate excretion in urine

Interactions

amphetamines, salicylates, sulfonylureas, tricyclic antidepressants: Decreased therapeutic blood level of ammonium chlorpropamide: Increased ammonium effects

Side Efect

CNS: Fever, headache
CV: Phlebitis or thrombosis extending from injection site
GI: Indigestion, nausea, severe hepatic dysfunction, vomiting
RESP: Hyperventilation
SKIN: Extravasation
Other: Injection site infection, irritation, or pain; hypovolemia; severe metabolic acidosis (with large doses)

Cautions

Before use, warm ammonium chloride solution to room temperature to dissolve crystals by placing infusion in warm water.

During I.V. use, keep sodium bicarbonate or sodium lactate nearby to treat overdose.

Infuse ammonium chloride slowly to avoid I.V. site pain and irritation.
WARNING Monitor patient for ammonia toxicity (arrhythmias, such as bradycardia; coma; irregular breathing; pallor; retching; seizures; diaphoresis; and twitching).

Watch for signs of metabolic acidosis, such as increased respirations, increased serum pH, restlessness, and diaphoresis.

Monitor serum bicarbonate level, urinalysis results, and renal and liver function test results as appropriate.

PATIENT SAFTY

Tell patient to eat potassium-rich such as bananas, oranges, cantaloupe, spinach, dried fruit, and potatoes, during therapy.

Category

Chemical class: Barbiturate
Therapeutic class: Anticonvulsant, sedativehypnotic

Pregnancy category: D

Controlled substance schedule: II

Indications

To produce preanesthesia sedation , ELIXIR,
Adults. 200 mg 1 to 2 hr before surgery. Children.2 to 6 mg/kg up to a maximum of 100 mg/dose. To produce sedation , ELIXIR,, I.V.OR I.M. INJECTION
Adults. 30 to 50 mg (may range from 15 to 120 mg) b.i.d. or t.i.d. Maximum I.V.: 1,000 mg/dose. Maximum I.M.: 500 mg/ dose. Children over age 6. 2 mg/kg daily in four divided doses. To treat insomnia , ELIXIR,
Adults.65 to 200 mg at bedtime for up to 2 wk. To induce a hypnotic state , ELIXIR,, I.V.OR I.M. INJECTION
Adults. 65 to 200 mg/dose. Maximum I.V.: 1,000 mg/dose. Maximum I.M.: 500 mg/ dose Children up to age 6. 2 to 3 mg/kg I.M. per dose. To manage seizures I.V.OR
I.M.INJECTION Use I.V. route only when other routes aren’t appropriate. For I.V. injection, use I.M. dose and inject slowly at 50 mg/min or less to prevent sudden respiratory depression, apnea, laryngospasm, or hypotension.
Adults. Usual: 65 to 500 mg to a maximum of 1,000 mg. Dosage for acute seizures is determined by response; 200to 500-mg doses are typically needed to control seizures. Children age 6 and over. 65 to 500 mg I.V. Children up to age 6. 3 to 5 mg/kg/dose. Route Onset Peak Duration P.O.* 60 min Unknown 10–12 hr I.V. Unknown Unknown 10–12 hr I.M. Unknown Unknown 10–12 hr

Mechanism of Action

Nonselectively acts on the CNS to depress the sensory cortex, decrease motor activity, alter cerebellar function, and produce drowsiness, sedation, and hypnosis. Appears to reduce wakefulness and alertness by acting in the thalamus, where it depresses the reticular activating system and interferes with impulse transmission from the periphery to the cortex. Produces CNS depressant effects ranging from mild sedation and anxiety reduction to anesthesia and coma, depending on the dose, route, and individual patient’s response.

Incompatibilities

Don’t mix amobarbital in solution with other .

Contraindications

Alcoholism, history of porphyria, history of sedative or barbiturate addiction, hypersensitivity to barbiturates, renal or hepatic disease, severe respiratory disease, sleep apnea, suicidal tendency, uncontrolled pain

Interactions

acetaminophen: Increased blood acetaminophen level and risk of hepatotoxicity antihistamines, CNS depressants, phenothiazines, tranquilizers: Increased CNS depression beta blockers, carbamazepine, clonazepam, corticosteroids, digitoxin, doxycycline, estrogens, griseofulvin, metronidazole, oral anticoagulants, oral contraceptives, phenylbutazones, quinidine, theophyllines, tricyclic antidepressants: Decreased blood levels and effects of these chloramphenicol: Inhibited amobarbital metabolism; enhanced chloramphenicol metabolism
MAO inhibitors: Increased serum level and sedative effects of amobarbital amobarbital sodium 72 * For capsules, elixir, and tablets.
methoxyflurane: Increased nephrotoxicity
phenytoin: Altered effects of phenytoin
rifampin: Decreased serum level and effects of amobarbital
valproic acid: Increased amobarbital effects
alcohol use: Increased serum level of amobarbital and additive CNS depressant effects

Side Efect

CNS: Agitation, anxiety, ataxia, CNS depression, confusion, dizziness, hallucinations, hangover, headache, hyperkinesia, insomnia, nightmares, nervousness, paradoxical stimulation, permanent neurologic deficit (with injection near nerve), psychiatric disturbance, somnolence, syncope, vertigo
CV: Bradycardia, hypotension, shock
EENT: Laryngospasm
GI: Constipation, diarrhea, epigastric pain, nausea, vomiting
RESP: Apnea, bronchospasm, hypoventilation, respiratory depression
SKIN: Exfoliative dermatitis, rash, StevensJohnson syndrome, urticaria
Other: Angioedema, gangrene of arm or leg from accidental injection into artery, injection site tissue damage and necrosis, physical and psychological dependence, potentially fatal withdrawal syndrome, tolerance

Cautions

Use amobarbital cautiously in patients with cardiac disease, debilitation, diabetes mellitus, fever, hyperthyroidism, severe anemia, shock, status asthmaticus, or uremia.

Administer by deep I.M. injection, preferably in large muscle.
WARNING To prevent tissue damage and necrosis at I.M. injection site, don’t give more than 5 ml of this highly alkaline drug at any one site. Know that accidental arterial injection may cause gangrene of the arm or leg.

During I.V. administration, closely monitor blood pressure, pulse, and respirations. Keep emergency equipment and nearby in case respiratory depression occurs.
WARNING Use I.V. route only when other routes aren’t appropriate.
WARNING Don’t administer solution after 30 minutes of exposure to air. Solution quickly becomes unstable because amobarbital sodium hydrolyzes in solution.

To prevent withdrawal symptoms, such as diaphoresis, insomnia, irritability, nightmares, and tremors, expect to taper amobarbital dosage gradually after long-term use, especially for epileptic patients.

PATIENT SAFTY

Advise patient to use caution when driving or doing tasks that require alertness.

Instruct patient not to use alcohol or other CNS depressants (unless prescribed) because they increase amobarbital’s effects.

Warn patient not to stop taking drug abruptly; withdrawal symptoms can occur.

Instruct patient to report severe dizziness, persistent drowsiness, rash, or skin lesions.

Explain that drug effects, such as drowsiness, may be less pronounced after a few days and when drug is taken with food.

Category

Chemical class: Dibenzoxazepine derivative
Therapeutic class: Tricyclic antidepressant

Pregnancy category: C

Indications

To relieve depression, including endogenous (long-term) depression and depression associated with anxiety and agitation Adults and children age 16 and over. Initial: 50 mg b.i.d. or t.i.d., increased to 100 mg b.i.d. or t.i.d. by end of first wk, if tolerated. Maintenance: If 300-mg daily dose is ineffective after 2-wk trial period, dosage increased to a maximum of 400 mg daily in divided doses. Inpatients may receive up to a maximum of 600 mg daily in divided doses. When effective dose is achieved, a single dose may be given at bedtime, not to exceed 300 mg.
DOSAGE ADJUSTMENT For elderly patients. Initial: 25 mg b.i.d. or t.i.d., increased to 50 mg b.i.d. or t.i.d. by end of first wk. Maintenance: 100 to 150 mg daily in divided doses, carefully increased to 300 mg daily as tolerated. When effective dose is achieved, a single dose may be given at bedtime, not to exceed 300 mg. Route Onset Peak Duration P.O. 2–3 wk Unknown Unknown

Mechanism of Action

Blocks serotonin and norepinephrine reuptake by adrenergic nerves, thus raising serotonin and norepinephrine levels at nerve synapses. This action may elevate mood and reduce depression. Normally, when an impulse reaches adrenergic nerves, they release serotonin and norepinephrine from their storage sites. Some serotonin and norepinephrine reach receptor sites on target tissues. The majority is taken back into the nerves and stored by the reuptake mechanism.

Contraindications

Acute recovery phase after MI, hypersensitivity to amoxapine or its components, MAO inhibitor therapy within 14 days

Interactions

anticholinergics, epinephrine, norepinephrine: Increased effects of these barbiturates: Decreased amoxapine level carbamazepine: Decreased serum amoxapine level; increased serum carbamazepine level, increasing its therapeutic and toxic effects cimetidine, disulfiram, fluoxetine, fluvoxamine, haloperidol, H2-receptor antagonists, methylphenidate, oral contraceptives, paroxetine, phenothiazines, sertraline: Increased blood amoxapine level clonidine, guanethidine, other antihypertensives: Decreased antihypertensive effects dicumarol: Increased anticoagulant effect levodopa: Decreased levodopa absorption; agitation, hypertension, sinus tachycardia, sympathetic hyperactivity
MAO inhibitors: Possibly seizures and death thyroid replacement : Arrhythmias and increased antidepressant effects
alcohol use: Increased CNS depression smoking: Decreased amoxapine effects

Side Efect

CNS: Agitation, anxiety, ataxia, chills, confusion, dizziness, drowsiness, excitement, extrapyramidal reactions, fatigue, fever, headache, insomnia, nervousness, nightmares, paresthesia, restlessness, sedation, seizures, stroke, syncope, tremor, weakness
CV: Atrial arrhythmias, heart block, heart failure, hypertension, hypotension, MI, palpitations, tachycardia
EENT: Blurred vision, dry mouth, increased salivation, nasal congestion, taste perversion, tinnitus
ENDO: Gynecomastia, increased or decreased blood glucose level, increased prolactin level, syndrome of inappropriate ADH secretion
GI: Anorexia, constipation, diarrhea, elevated liver function test results, flatulence, increased appetite, nausea, vomiting
GU: Impotence, libido changes, menstrual irregularities, testicular swelling, urinary hesitancy, urine retention
HEME: Agranulocytosis, leukopenia
SKIN: Diaphoresis, flushing, photosensitivity, pruritus, rash
Other: Weight gain or loss; withdrawal symptoms, such as headache, nausea, nightmares, and vertigo

Cautions

WARNING Don’t give an MAO inhibitor within 14 days of amoxapine.

To avoid withdrawal, don’t stop drug abruptly.

Watch patients closely (especially children, adolescents, and young adults), for suicidal tendencies, particularly when therapy starts and dosage changes, because depression may worsen temporarily during these times.

PATIENT SAFTY

Advise patient to take amoxapine at bedtime if daytime sedation occurs.

Caution patient that stopping amoxapine abruptly may cause withdrawal symptoms.

Urge patient to avoid alcohol because it can potentiate amoxapine’s effects.

Tell patient to report adverse effects of amoxapine.

Instruct patient to take drug with food to prevent GI upset.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes and particularly if patient is a child, teenager, or young adult.

Category

Chemical class: Aminopenicillin
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat ear, nose, throat, GU tract, skin, and soft-tissue infections caused by susceptible gram-positive and gramnegative organisms , CHEWABLE , ORAL SUSPENSION, PEDIATRIC DROPS, POWDER OR FOR ORAL SUSPENSION, Adults and children weighing 20 kg (44 lb) or more.250 mg every 8 hr; for severe infections, 500 mg every 8 hr or 875 mg every 12 hr. Children age 12 wk and over weighing less than 20 kg. 20 mg/kg daily in divided doses every 8 hr; for severe infections, 40 to 45 mg/kg/day in divided doses every 8 hr. Children under age 12 wk. 30 mg/kg/ day in divided doses every 12 hr. To treat tonsillitis or pharyngitis caused by Streptococcus pyogenes (MOXATAG) Adults and children age 12 and over. 775 mg once dailyfor 10 days, taken within 1 hr of finishing a meal. To treat lower respiratory tract infections caused by susceptible gram-positive and gram-negative organisms , CHEWABLE , ORAL SUSPENSION, PEDIATRIC DROPS, POWDER OR FOR ORAL SUSPENSION, Adults and children weighing 20 kg or more.875 mg every 12 hr; for severe infections, 500 mg every 8 hr. Children age 12 wk and over weighing less than 20 kg. 40 to 45 mg/kg daily in divided doses every 8 hr. Children under age 12 wk. 30 mg/kg daily in divided doses every 12 hr. To treat gonorrhea and acute uncomplicated anogenital and urethral infections caused by susceptible strains of grampositive and gram-negative organisms , CHEWABLE , ORAL SUSPENSION, POWDER OR FOR ORAL SUSPENSION, Adults and postpubertal children.3 g as a single dose. Prepubertal children age 2 and over. 50 mg/kg of amoxicillin plus 25 mg/kg of pro-benecid as a single dose. As adjunct to eradicate Helicobacter pylori to reduce risk of duodenal ulcer recurrence , CHEWABLE , ORAL SUSPENSION, POWDER OR FOR ORAL SUSPENSION,
Adults. 1 g every 12 hr with 500 mg of clarithromycin every 12 hr and 30 mg of lansoprazole every 12 hr for 14 days. Or, 1 g every 8 hr with 30 mg of lansoprazole every 8 hr for 14 days. To prevent bacterial endocarditis before dental, oral, or upper respiratory tract procedures , CHEWABLE , ORAL SUSPENSION, POWDER OR FOR ORAL SUSPENSION, Adults and children weighing 20 kg or more. 2 g 1 hr before procedure. Children weighing less than 20 kg. 50 mg/ kg 1 hr before procedure. Route Onset Peak Duration P.O. Unknown Unknown 6–8 hr

Mechanism of Action

Kills bacteria by binding to and inactivating penicillin-binding proteins on the inner bacterial cell wall, weakening the bacterial cell wall and causing lysis.

Contraindications

Hypersensitivity to amoxicillin or its components

Interactions

allopurinol: Increased risk of rash chloramphenicol, erythromycins, sulfonamides, tetracyclines: Reduced bactericidal effect of amoxicillin methotrexate: Increased risk of methotrexate toxicity oral contraceptives with estrogen: Possibly reduced effectiveness of contraceptive probenecid: Increased amoxicillin effects

Side Efect

CNS: Agitation, anxiety, behavior changes, confusion, dizziness, insomnia, reversible hyperactivity, seizures
CV: Hypersensitivity vasculitis
EENT: Black, hairy tongue; mucocutaneous candididasis; tooth discoloration
GI: Diarrhea, diarrhea related to Clostridium difficile, elevated liver enzymes, hemorrhagic or pseudomembranous colitis, jaundice, hepatic dysfunction, nausea, vomiting
GU: Crystalluria, vaginal mycosis
HEME: Agranulocytosis, anemia (including hemolytic anemia), eosinophilia, granulocytosis, leukopenia, thrombocytopenia, thrombocytopenic purpura
SKIN: Erythema multiforme, erythematous maculopapular rash, generalized exanthematous pustulosis, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Allergic reaction, anaphylaxis, serum sicknesslike reaction (such as arthralgia, arthritis, fever, myalgia, rash, and urticaria)

Cautions

Patients with mononucleosis shouldn’t receive amoxicillin because this class of may cause an erythematous rash.

Use drug cautiously in patients with hepatic impairment. Monitor hepatic and renal function and CBC, as ordered, in patients on prolonged therapy. Also use cautiously in breast-feeding and elderly patients.

Expect to start therapy before culture and sensitivity test results are known.

Be aware that chewable tablets and tablets for oral suspension contain phenylalanine.

Don’t confuse amoxicillin tablets with amoxicillin tablets for oral suspension (DisperMox). They’re not interchangeable.
WARNING If allergic reaction occurs, stop amoxicillin immediately and provide emergency care as indicated and ordered.

Monitor patient closely for diarrhea, which may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber, expect to withhold amoxicillin, and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Expect treatment that lasts at least 10 days for hemolytic streptococci infections.

Monitor patient for superinfection. If it occurs, expect to discontinue drug and provide treatment as ordered.

PATIENT SAFTY

Tell patient to refrigerate reconstituted suspension and to shake well before each use.

When amoxicillin suspension is prescribed for a child, instruct parents to place it directly on child’s tongue to swallow. If this doesn’t work, tell parents to mix dose of suspension with formula or cold drink (milk, fruit juice, ginger ale, water) and have child drink it immediately.

Instruct patient using DisperMox tablets to place one tablet and about 2 teaspoonfuls of water in a glass, drink entire mixture, add more water to the glass, and drink again to ensure delivery of full dose.

Tell patient to chew or crush chewable tablets and not to swallow them whole.

To prevent infection from recurring, urge patient to take amoxicillin for full length of time prescribed, even if he feels better.

Teach patient to report

Side Efect

and notify prescriber if infection worsens or doesn’t improve after 72 hours.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and may be serious, requiring prompt treatment.

Category

Chemical class: Sympathomimetic amine
Therapeutic class: CNS stimulant

Pregnancy category: C

Controlled substance schedule: II

Indications

To treat attention deficit hyperactivity disorder (ADHD)

ORALL

(LIQUADD) Children ages 3 to 6. Initial: 2.5 mg daily. amphetamine sulfate 76 Increased by 2.5 mg daily at 1-wk intervals until desired response occurs. Children age 6 and over. Initial: 5 mg daily or b.i.d. Increased by 5 mg daily at 1-wk intervals until desired response occurs. Children age 6 and over.Initial: 5 mg daily or b.i.d. Increased by 5 mg daily at 1-wk intervals until desired response occurs. Usual: 0.1 to 0.5 mg/kg daily. Children ages 3 to 5. Initial: 2.5 mg daily. Increased by 2.5 mg daily at 1-wk intervals until desired response occurs. Usual: 0.1 to 0.5 mg/kg daily. To treat narcolepsy

ORALL

(LIQUADD) Adults and children age 12 and over.Initial: 10 mg daily. Increased by 10 mg daily at 1wk intervals until desired response occurs. Children ages 6 to 12. Initial: 2.5 mg b.i.d. Increased by 5 mg daily at 1-wk intervals until desired response occurs. Adults and children age 12 and over.Initial: 10 mg daily. Increased by 10 mg daily at 1wk intervals until desired response occurs. Children ages 6 to 12. Initial: 2.5 mg b.i.d. Increased by 5 mg daily at 1-wk intervals until desired response occurs or adult dosage is reached to a maximum of 60 mg daily.

Mechanism of Action

May produce its CNS stimulant effects by facilitating release and blocking reuptake of norepinephrine at adrenergic nerve terminals and by direct stimulation of alpha and beta receptors in the peripheral nervous system. It also releases and blocks reuptake of dopamine in limbic regions of the brain. The drug’s main action appears to be in the cerebral cortex and, possibly, the reticular activating system. These actions cause decreased motor restlessness, increased alertness, and diminished drowsiness and fatigue. Its peripheral actions include increased blood pressure and mild bronchodilation and respiratory stimulation.

Contraindications

Advanced arteriosclerosis, agitation (for narcolepsy treatment), glaucoma, history of drug abuse, hypersensitivity or idiosyncratic reaction to sympathomimetic amines, hyperthyroidism, MAO inhibitor therapy within 14 days, moderate to severe hypertension, symptomatic cardiovascular disease

Interactions

adrenergic blockers: Inhibited adrenergic blockade acetazolamide, alkalinizers (such as sodium bicarbonate), some thiazides: Increased blood level and effects of amphetamine antihistamines: Possibly reduced sedation from antihistamine antihypertensives: Possibly decreased antihypertensive effects chlorpromazine: Inhibited CNS stimulant effects of amphetamine ethosuximide: Possibly delayed ethosuximide absorption GI acidifiers (such as ascorbic acid), reserpine: Decreased amphetamine absorption guanethidine: Decreased antihypertensive effect and decreased amphetamine absorption
haloperidol: Decreased CNS stimulation lithium carbonate: Possibly decreased anorectic and stimulant effects of amphetamine
MAO inhibitors: Potentiated effects of amphetamine; possibly hypertensive crisis meperidine: Increased analgesia methenamine: Increased urine excretion and decreased effects of amphetamine norepinephrine: Possibly increased adrenergic effect of norepinephrine phenobarbital,
phenytoin: Synergistic anticonvulsant action propoxyphene: Increased CNS stimulation, potentially fatal seizures tricyclic antidepressants: Possibly enhanced antidepressant effects and decreased effects of amphetamine urinary acidifiers (such as ammonium chloride and sodium acid phosphate): Increased amphetamine excretion and decreased amphetamine blood level and effects veratrum alkaloids: Decreased hypotensive effect acidic fruit juices: Decreased amphetamine absorption

Side Efect

CNS: Anxiety, dizziness, dyskinesia, dysphoria, euphoria, exacerbation of motor and phonic tics and Tourette’s syndrome, cinations, headache, insomnia, overstimulation, paranoia, psychotic episodes, restlessness, tremor
CV: Cardiomyopathy, hypertension, palpitations, tachycardia
EENT: Dry mouth, unpleasant taste
GI: Anorexia, constipation, diarrhea
GU: Impotence, libido changes
SKIN: Urticaria
Other: Weight loss

Cautions

Keep in mind that when symptoms of ADHD occur with acute stress reactions, treatment with amphetamines usually isn’t indicated.
WARNING To prevent hypertensive crisis, don’t give amphetamine during or for up to 14 days after MAO therapy.

Give first dose when patient awakens and additional doses at 4to 6-hour intervals.

Be aware that 5 ml of oral solution contains 5 mg of dexamphetamine.

If patient has bothersome adverse reactions, such as insomnia and anorexia, expect to decrease dosage. To minimize insomnia, administer drug earlier in day.

Be alert for evidence of long-term amphetamine abuse, such as severe dermatoses, marked insomnia, irritability, hyperactivity, and personality changes. If patient suddenly stops drug after longterm, high-dose regimen, watch for extreme fatigue and depression.

PATIENT SAFTY

Instruct breast-feeding patient to avoid breast-feeding during amphetamine therapy because drug is excreted in breast milk.

Teach patient to take first dose on awakening and subsequent doses at 4to 6-hour intervals. Tell him not to take last dose late in evening because insomnia may occur.

Inform patient or caregiver that each 5 ml of oral solution contains 5 mg of dexamphetamine. Advise patient to use a calibrated measuring device for accurate dose.

Urge patient to avoid hazardous activities until drug’s effects are known.

Advise patient not to take amphetamine with acidic fruit juice because doing so decreases drug absorption.

Explain drug’s abuse potential, and caution against altering dosage unless prescribed.

Category

Chemical class: Amphoteric polyene macrolide
Therapeutic class: Antifungal

Pregnancy category: B

(I.V.); C (oral suspension)

Indications

To treat severe fungal infections, using amphotericin B
IV: Adults and adolescents. Initial: 1-mg test dose in 20 ml of D5W infused over 20 to 30 min; if test dose is tolerated, then 0.25 to 0.3 mg/kg daily prepared as a 0.1 mg/ml infusion, given over 2 to 6 hr. Increased in 5to 10-mg increments up to 50 mg daily, based on patient tolerance and infection severity, not to exceed a total daily dose of 1.5 mg/kg. Maximum: 50 mg daily infused over 2 to 6 hr. Children.Initial: 0.25 mg/kg daily in D5W infused over 6 hr; then increased in 0.125to 0.25-mg/kg increments daily or every other day as tolerated. Maximum: 1 mg/kg or 30 mg/m2of body surface daily. To treat oral candidiasis, using amphotericin B ORAL SUSPENSION Adults and children.1 ml (100 mg) q.i.d. for 14 days. To treat aspergillosis, using amphotericin B cholesteryl sulfate complex amphotericin B 78
IV: Adults and children. Test dose of 1.6 to 8.3 mg in 10 ml of D5W infused over 15 to 30 min; if test dose is tolerated, then 3 to 4 mg/kg once daily infused at 1 mg/kg/hr. To treat invasive amphotericin Bresistant fungal infections, using amphotericin B lipid complex
IV: Adults and children. 5 mg/kg daily infused at 2.5 mg/kg/hr. To treat severe aspergillosis, candidiasis, or cryptococcosis, using amphotericin B liposomal complex
IV: Adults and children. 3 to 5 mg/kg daily infused over 2 hr. Infusion time may be decreased to 1 hr if tolerated or increased if patient experiences discomfort. To treat leishmaniasis, using amphotericin B liposomal complex
IV: Immunocompetent adults and children. 3 mg/kg daily on days 1 through 5 and on days 14 and 21, infused over 2 hr. Infusion time may be decreased to 1 hr if tolerated or increased if patient has discomfort. Immunocompromised adults and children. 4 mg/kg daily on days 1 through 5 and days 10, 17, 24, 31, and 38 infused over 2 hr. Infusion time may be decreased to 1 hr if tolerated or increased if patient has discomfort. To treat presumed fungal infections in patients with febrile neutropenia, using amphotericin B lipid complex
IV: Adults and children. 3 mg/kg daily infused over 2 hr. Infusion time may be decreased to 1 hr if tolerated or increased if patient has discomfort. Route Onset Peak Duration I.V. Immediate Unknown Unknown

Mechanism of Action

Binds to sterols in fungal cell plasma membranes, which changes membrane permeability and allows loss of potassium and small molecules from cells. This action results in cell impairment or death.

Incompatibilities

Don’t reconstitute amphotericin B with diluents other than those recommended because solutions with sodium chloride or bacteriostatic agents (such as benzyl alcohol) may cause drug precipitation.

Contraindications

Hypersensitivity to amphotericin B or its components

Interactions

antineoplastics: Increased risk of bronchospasm, hypotension, and nephrotoxicity corticosteroids, corticotropin: Increased risk of hypokalemia and cardiac dysfunction cyclosporine, nephrotoxic : Increased risk of nephrotoxicity digitalis glycosides: Possibly hypokalemia and more severe digitalis toxicity flucytosine: Possibly increased flucytosine toxicity leukocyte transfusion: Possibly dyspnea, hypoxemia, and pulmonary infiltrates skeletal muscle relaxants: Possibly hypokalemia and increased muscle relaxation zidovudine: Possibly myelotoxicity and nephrotoxicity

Side Efect

CNS: Fever, headache, shaking chills, tiredness, weakness
CV: Chest pain, hypotension, irregular heartbeat
EENT: Difficulty swallowing, pharyngitis
GI: Abdominal pain, anorexia, diarrhea, hepatic failure, indigestion, nausea, vomiting
GU: Decreased or increased urine output, impaired renal function
HEME: Anemia, leukopenia, thrombocytopenia, unusual bleeding or bruising
MS: Arthralgia, muscle spasms, myalgia
RESP: Apnea, dyspnea, hypoxia, pulmonary edema, tachypnea
SKIN: Flushing, jaundice, maculopapular rash, pruritus and redness especially around ears, urticaria
Other: Anaphylaxis, hypocalcemia, hypokalemia, hypomagnesemia, infusion site pain and thrombophlebitis

Cautions

To prepare amphotericin B, add 10 ml of sterile water for injection without a bacteriostatic agent to vial containing 50 mg of amphotericin B. For I.V. infusion, dilute solution containing 5 mg/ml to 0.1 mg/ml by adding 1 ml (5 mg) of solution to 49 ml of D5W with a pH above 4.2.

Before using D5W to dilute amphotericin B solution, determine the injection’s pH aseptically. If pH is below 4.2, follow manufacturer’s instructions for buffering it.

Because reconstituted amphotericin B is a colloidal suspension, avoid using in-line membrane filter or use one with a mean pore diameter of more than 1 micron to prevent significant drug removal.

To prepare amphotericin B cholesteryl sulfate complex, reconstitute with sterile water for injection. Using a sterile syringe and 20G needle, rapidly add 10 or 20 ml sterile water for injection to a 50or 100mg vial, respectively, to obtain a solution containing 5 mg of amphotericin B per milliliter. Shake gently by hand, rotating vial until solids are dissolved; fluid may be clear or opalescent. For infusion, further dilute reconstituted solution to about 0.6 mg/ml. Don’t filter solution or use an in-line filter. Flush existing line with D5W or use a separate line.

To prepare amphotericin B lipid complex, shake vial gently until you see no yellow sediment. Using an 18G needle, withdraw prescribed dose from required number of vials into one or more 20-ml syringes. Replace needle with 5-micron filter needle supplied with each vial. Empty syringe contents into bag of D5W so that final concentration is 1 mg/ml. Expect to use a concentration of 2 mg/ml for children and patients with cardiovascular disease. Before infusion, shake bag until contents are mixed thoroughly. Flush existing line with D5W, or use a separate line. Don’t use an in-line filter. If infusion exceeds 2 hours, shake infusion bag every 2 hours.

To prepare amphotericin B liposomal complex, add 12 ml sterile water for injection (without bacteriostatic agent) to each 50-mg vial to achieve a concentration of 4 mg amphotericin B per milliliter. Immediately shake vial vigorously for at least 30 seconds until all particles completely disperse. Withdraw prescribed dose of amphotericin B liposomal complex suspension. Then use a 5-micron filter to inject it into D5W to provide a final concentration of 1 to 2 mg/ml. Expect to use a lower concentration (0.2 to 0.5 mg/ ml) for infants and young children. Flush existing line with D5W, or use a separate line.You may use an in-line filter with a mean pore diameter of at least 1 micron.

To help minimize fever and shaking chills, expect to give an antipyretic, antihistamine, meperidine, or corticosteroid just before infusing amphotericin B.

Before giving amphotericin B oral suspension, shake well. Drop suspension on tongue with calibrated dropper. Then tell patient to swish suspension in mouth for as long as possible before swallowing. If drug must be swabbed on, use a nonabsorbent swab.

Give amphotericin B oral suspension between meals to permit prolonged contact with oral lesions.

Assess I.V. insertion site regularly to detect extravasation of amphotericin B, which may cause severe local irritation. To minimize local thrombophlebitis, plan to add heparin to infusion or expect to administer amphotericin on alternate days, which also may help prevent anorexia. Alternateday dose shouldn’t exceed 1.5 mg/kg.

Monitor renal function because of the risk of renal impairment. Plan to obtain serum creatinine level every other day while amphotericin B dosage is increasing and then at least twice weekly during therapy. If serum creatinine or BUN level increases significantly, expect to stop amphotericin B until renal function improves. Know that a cumulative dose of more than 4 g may cause irreversible renal dysfunction.

Expect to monitor CBC and platelet count weekly during therapy to detect adverse hematologic effects. Also monitor serum calcium, magnesium, and potassium levels twice weekly to detect abnormalities.

Use reconstituted amphotericin B within 24 hours if stored at room temperature, 1 week if refrigerated. Use reconstituted amphotericin B cholesteryl sulfate complex within 24 hours. Use amphotericin B lipid complex within 6 hours if stored at room temperature, 48 hours if refrigerated. Use diluted amphotericin B liposomal complex within 24 hours if refrigerated, but begin infusion within 6 hours.

PATIENT SAFTY

Instruct patient to shake bottle of oral suspension well before each dose; to drop amphotericin B 80 suspension directly on his tongue using calibrated dropper; and then to swish suspension in his mouth for as long as possible before swallowing. If prescriber orders drug to be swabbed onto oral lesions, tell patient to use nonabsorbent swab. Instruct him to take drug four times a day (between meals and at bedtime).

Tell patient to notify prescriber if he develops local irritation, if existing symptoms worsen or return, or if new symptoms arise.

Category

Chemical class: Semisynthetic aminopenicillin
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat GI infections and genitourinary infections (other than gonorrhea) caused by susceptible strains of Shigella, Salmonella typhi and other species, Escherichia coli, Proteus mirabilis, and enterococci , ORAL SUSPENSION,

IV

,

IM

Adults and children weighing 20 kg (44 lb) or more. 500 mg P.O. every 6 hr or 250 to 500 mg I.V. or I.M. every 6 hr. Children weighing less than 20 kg. 50 to 100 mg/kg daily in divided doses P.O. every 6 hr or 12.5 mg/kg I.V. or I.M. every 6 hr. To treat gonorrhea caused by susceptible strains of non–penicillinase-producing Neisseria gonorrhoeae , ORAL SUSPENSION Adults and children.3.5 g as a single dose with 1 g of probenecid.
IV:,
I.M.INJECTION Adults and children weighing 45 kg (99 lb) or more. 500 mg every 6 hr. Children weighing less than 40 kg (88 lb). 50 mg/kg daily in divided doses every 6 to 8 hr. To treat respiratory tract infections caused by susceptible strains of nonpenicillinase–producing Haemophilus influenzae, staphylococci, and streptococci, including Streptococcus pneumoniae , ORAL SUSPENSION,
IV:,
I.M.INJECTION Adults and children weighing 40 kg or more.250 to 500 mg I.V. or I.M. every 6 to 8 hr. Adults and children weighing 20 kg or more. 250 mg P.O. every 6 hr. Children weighing less than 40 kg. 25 to 50 mg/kg daily I.V. or I.M. in divided doses every 6 to 8 hr. Children weighing less than 20 kg. 50 mg/ kg daily P.O. in divided doses every 6 or 8 hr or 12.5 mg/kg I.V. or I.M. every 6 hr. To treat septicemia
IV:,
I.M.INJECTION
Adults.8 to 14 g I.V. daily in divided doses every 3 to 4 hr for at least 3 days; then I.M. Children.150 to 200 mg/kg daily I.V. in divided doses every 3 to 4 hr for at least 3 days; then I.M. To prevent bacterial endocarditis from dental, oral, or upper respiratory tract procedures
IV:,
I.M.INJECTION
Adults.2 g within 30 min of procedure Children. 50 mg/kg within 30 min of procedure To treat bacterial meningitis caused by susceptible strains of Neisseria meningitidis
IV:,
I.M.INJECTION
Adults.8 to 14 g daily or 150 to 200 mg/kg daily I.V. in equally divided doses every 3 to 4 hr for at least 3 days; then I.M. at same dosage and schedule. Children.100 to 200 mg/kg daily I.V. in equally divided doses every 3 to 4 hr for at least 3 days; then I.M. at same dosage and schedule. To treat listeriosis
IV:,
I.M.INJECTION Adults and children weighing 20 kg or more. 50 mg/kg every 6 hr. Children weighing less than 20 kg. 12.5 mg/kg every 6 hr. Route Onset Peak Duration I.V. Immediate Unknown Unknown

Mechanism of Action

Inhibits bacterial cell wall synthesis. The rigid, cross-linked cell wall is assembled in several steps. Ampicillin exerts its effects on susceptible bacteria in the final stage of the cross-linking process by binding with and inactivating penicillin-binding proteins (enzymes responsible for linking the cell wall strands). This action causes bacterial cell lysis and death.

Incompatibilities

Don’t mix ampicillin and any aminoglycoside in the same I.V. bag, bottle, or tubing; otherwise, both will be inactivated. If patient must receive both , administer them in separate sites at least 1 hour apart.

Contraindications

Hypersensitivity to any penicillin, infection caused by penicillinase-producing organism

Interactions

allopurinol: Increased risk of rash, particularly in hyperuricemic patient aminoglycosides: Possibly inactivated action of aminoglycoside and ampicillin when given together heparin, oral anticoagulants: Increased risk of bleeding oral contraceptives: Possibly reduced contraceptive effectiveness and breakthrough bleeding probenecid: Possibly increased serum ampicillin level and ampicillin toxicity tetracyclines: Possibly impaired action of ampicillin

Side Efect

CNS: Chills, fatigue, fever, headache, malaise
CV: Chest pain, edema, thrombophlebitis
EENT: Epistaxis, glossitis, laryngeal stridor, mucocutaneous candidiasis, stomatitis, throat tightness
GI: Abdominal distention, diarrhea, diarrhea related to Clostridium difficile, enterocolitis, flatulence, gastritis, nausea, pseudomembranous colitis, vomiting
GU: Dysuria, urine retention, vaginal candidiasis
HEME: Agranulocytosis, anemia, eosinophilia, leukopenia, thrombocytopenia, thrombocytopenic purpura
SKIN: Erythema multiforme; erythematous, mildly pruritic maculopapular rash or other types of rash; exfoliative dermatitis; pruritus; urticaria
Other: Anaphylaxis, facial edema, injection site pain

Cautions

Avoid giving ampicillin to patients with mon-nucleosis because of increased risk of rash.

Expect to give ampicillin for 48 to 72 hours after patient becomes asymptomatic. For streptococcal infection, expect to give ampicillin for at least 10 days after cultures show streptococcal eradication to reduce risk of rheumatic fever or glomerulonephritis.

To dilute ampicillin for I.M. use, add (depending on manufacturer) 1.2 ml of sterile water or bacteriostatic water for injection to each 125-mg vial, 1 ml of diluent to each 250-mg vial, 1.8 ml of diluent to each 500-mg vial, 3.5 ml of diluent to each 1-g vial, or 6.8 ml of diluent to each 2-g vial.

To dilute ampicillin for intermittent infusion, add 5 ml of sterile water or bacteriostatic water for injection to each 125-, 250-, or 500-mg vial or 7.4 to 10 ml of diluent to each 1or 2-g vial. Infuse in suitable diluent at less than 30 mg/ml.
WARNING Infuse I.V. solution for 3 to 5 minutes for each 125 or 500 mg or 10 to 15 minutes for each 1 or 2 g. More rapid infusion may cause seizures.

Monitor patient closely for anaphylaxis, which may be life-threatening. Patients at greatest risk are those with a history of multiple allergies, hypersensitivity to cephalosporins, or a history of asthma, hay fever, or urticaria.
WARNING In an anaphylactic reaction, stop drug, notify prescriber immediately, and provide immediate treatment with epinephrine, airway management, oxygen, and I.V. corticosteroids, as needed.

Notify prescriber if patient has evidence of ampicillin 82 superinfection; expect to stop drug and provide appropriate treatment.

If long-term or high-dose ampicillin therapy is required, closely monitor results of renal and liver function tests and CBCs.

Monitor patient closely for diarrhea, which may be pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold ampicillin and administer fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

PATIENT SAFTY

Stress the importance of taking the full course of ampicillin exactly as prescribed.

Tell patient to take dose with 8 oz of water 30 minutes before or 2 hours after meals.

Instruct patient to shake suspension well before each use, keep bottle tightly closed between uses, and discard unused portion after 14 days if refrigerated or 7 days if stored at room temperature.

Review signs of allergic reaction; if they occur, tell patient to hold next ampicillin dose and contact prescriber immediately.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools may occur 2 or more months after antibiotic therapy and may be serious, requiring prompt treatment.

Category

Chemical class: Nitrite ester
Therapeutic class: Antianginal

Pregnancy category: C

Indications

To treat acute attacks of angina pectoris CRUSHABLE AMPULES
Adults.1 ampule (0.18 or 0.3 ml) inhaled and repeated in 3 to 5 min, if needed. Route Onset Peak Duration Inhalation 10–30 sec Unknown 3–5 min

Mechanism of Action

After inhalation, is absorbed by pulmonary alveoli, which causes relaxation of vascular smooth-muscle cells, dilation of large coronary blood vessels, decreased systemic vascular resistance, decreased venous return to the heart, reduced afterload, decreased cardiac ouput, and subsequent relief of angina.

Contraindications

Hypersensitivity to amyl nitrite, its components, or nitrates

Interactions

aspirin: Increased serum level and action of amyl nitrite calcium channel blockers: Possibly severe symptomatic hypotension
sildenafil: Increased risk of hypotension sympathomimetics: Possibly decreased antianginal effects and severe hypotension and tachycardia
alcohol use: Increased risk of severe hypotension and cardiovascular collapse

Side Efect

CNS: Dizziness, headache, restlessness, syncope, weakness
CV: Orthostatic hypotension, tachycardia
GI: Fecal incontinence, nausea, vomiting
GU: Urinary incontinence
HEME: Hemolytic anemia, methemoglobin-emia
SKIN: Face and neck flushing, pallor, rash

Cautions

Use amyl nitrite cautiously in elderly patients and patients with cerebral hemorrhage, glaucoma, hyperthyroidism, recent head trauma or MI, or severe anemia.

Monitor blood pressure during and after drug administration. Also monitor cardiac function periodically in patients who use amyl nitrite regularly.
WARNING Stop drug and notify prescriber if evidence of overdose, such as bluish lips, fingernails, or palms; dizziness; fainting; extreme pressure in head; dyspnea; unusual tiredness or weakness; a weak or fast heartbeat; or increased methemoglobin level. Cyanosis may occur when methemoglobin level reaches 1.5 g/dl. More pronounced signs occur at 20 to 50 g/dl.

Expect to treat overdose with high-flow oxygen and I.V. methylene blue. If hypotension is severe, place patient head down. If he needs a vasopressor, avoid epinephrine; it may cause severe hypotension.

PATIENT SAFTY

Advise patient to store amyl nitrate in a tight container, protected from light.

Tell patient to crush ampule between finger and thumb, hold it to nostrils, and inhale 1 to 6 times.

Instruct patient to remain seated or supine during administration and to rise slowly afterward to prevent dizziness.

Inform patient that relief usually occurs in 1 to 5 minutes. If pain continues, he should repeat dose. If pain continues after another 5 minutes, he should seek emergency help.

Urge patient not to use any more drug than prescribed because of possible overdose.
WARNING Caution patient that drug is flammable and must be kept from flame and heat.

Inform patient that amyl nitrite commonly causes headaches. Tell him to notify prescriber if they’re severe or bothersome.

Category

Chemical class: Imidazoquinazolinone
Therapeutic class: Platelet count–reducing agent

Pregnancy category: C

Indications

To treat essential thrombocythemia
Adults.0.5 mg q.i.d. or 1 mg b.i.d. for 1 wk; then adjusted to lowest dose that keeps platelet count below 600,000/mm3or within normal range. Shouldn’t be increased by more than 0.5 mg daily in any 1 wk. Maximum: 10 mg daily or 2.5 mg in a single dose.
DOSAGE ADJUSTMENT For patients with moderate hepatic impairment, 0.5 mg daily for at least 1 wk, increased as needed by no more than 0.5 mg daily in any 1-wk period.

Mechanism of Action

May decrease megakaryocyte hypermaturation (bone marrow cells from which platelets form), reducing platelet count. Higher doses may inhibit platelet aggregation. Route Onset Peak Duration P.O. 7–14 days Unknown Up to 4 days

Contraindications

Hypersensitivity to anagrelide, severe hepatic impairment

Interactions

amrinone, cilostazol, enoximone, milrinone, olprinone: Increased effects of these ; possible risk of increased adverse effects aspirin: Possibly increased risk of bleeding sucralfate: Possibly interference with anagrelide absorption

Side Efect

CNS: Amnesia, asthenia, chills, confusion, depression, dizziness, fever, headache, insomnia, malaise, nervousness, paresthesia, seizures, somnolence, stroke, syncope, weakness
CV: Angina, arrhythmias, edema, heart failure, hypertension, MI, orthostatic hypotension, palpitations, tachycardia, vasodilation
EENT: Amblyopia, diplopia, epistaxis, rhinitis, sinusitis, stomatitis, tinnitus, vision or visual field abnormality
GI: Abdominal pain, anorexia, constipation, diarrhea, elevated liver function test results, eructation, flatulence, gastric and duodenal ulceration, gastritis, GI hemorrhage, hepatotoxicity, indigestion, melena, nausea, pancreatitis, vomiting
GU: Dysuria, hematuria, renal failure
HEME: Anemia, hemorrhage, thrombocytopenia
MS: Arthralgia, back pain, leg cramps, myalgia, neck pain
RESP: Allergic alveolitis, asthma, bronchitis, dyspnea, eosinophilic pneumonia, interstitial pneumonitis, lung infiltrations, pneumonia
SKIN: Alopecia, ecchymosis, photosensitivity, pruritus, rash, urticaria
Other: Dehydration, flulike symptoms, generalized body pain, lymphadenoma

Cautions

Use anagrelide cautiously in patients with heart disease because it may cause cardiovascular problems, such as heart failure. anagrelide hydrochloride 84 Use drug cautiously in patients with renal insufficiency (serum creatinine level 2 mg/ dl or more) or hepatic dysfunction (liver function tests more than 1.5 times normal) because of the increased risk of nephrotoxicity and hepatotoxicity.

Determine whether patient takes aspirin before starting anagrelide therapy and, if so, monitor patient closely because bleeding risk may be higher when aspirin and anagrelide are taken concurrently.

To assess efficacy and prevent thrombocytopenia, expect to monitor platelet count every 2 days for first week, then at least weekly until reaching lowest effective dose.

While platelet count is declining (usually during first 2 weeks of therapy), assess WBC count and hemoglobin, AST, ALT, creatinine, and BUN levels to detect abnormalities.

Monitor blood pressure to detect orthostatic hypotension.

PATIENT SAFTY

Stress need to return for laboratory tests, such as platelet counts, to monitor anagrelide’s effectiveness and adjust its dosage.

Tell patient to keep drug bottle tightly capped and to protect drug from light.

Urge patient to ask prescriber before taking aspirin or aspirin-containing products.

Category

Chemical class: Recombinant human interleukin-1 receptor antagonist
Therapeutic class: Antirheumatic

Pregnancy category: B

Indications

To reduce signs and symptoms and slow structural damage in moderate to severe active rheumatoid arthritis in patients who have not responded to diseasemodifying antirheumatics SUBCUTANEOUS INJECTION
Adults. 100 mg daily.
DOSAGE ADJUSTMENT Interval reduced to every other day in severe renal insufficiency or end-stage renal disease (creatinine clearance less than 30 ml/min/1.73 m2).

Mechanism of Action

Inhibits the binding of interleukin-1 (IL-1) to its type 1 receptor, blocking its activity. Inflammatory stimuli prompt T cells to release IL-1, a mediator of inflammation, pain, and stiffness in rheumatoid arthritis.

Contraindications

Active infection; hypersensitivity to anakinra, its components, or Escherichia coli– derived proteins

Interactions

etanercept, infliximab, and other that block tumor necrosis factor: Increased risk of serious infection live-virus vaccines Possibly decreased antibody response to vaccine, potential for infection with live virus

Side Efect

CNS: Headache
EENT: Sinusitis
GI: Abdominal pain, diarrhea, nausea
HEME: Neutropenia
MS: Bone and joint infections
RESP: Pneumonia, upper respiratory tract infection Skin: Cellulitis
Other: Flulike symptoms; hypersensitivity reaction; injection site ecchymosis, erythema, inflammation, pain, and pruritus; malignancies; positive results for antianakinra antibodies; serious infections

Cautions

Expect to obtain baseline neutrophil count before therapy and to monitor neutrophil count every month for 3 months and every 3 months for up to 1 year.

Discard solution if it contains particles or is discolored. Use prefilled syringe and needles to administer drug. Don’t shake syringe; allow time for solution to clear if it becomes foamy.

Give drug about the same time each day.
WARNING Anakinra isn’t recommended for patients with active infections. Monitor patient for evidence of infection, such as fever, chills, sore throat, and mouth sores, before and during therapy because drug increases the risk of infections, such as cellulitis, pneumonia, and bone and joint infections. Notify prescriber if signs are present. Patients with asthma and those receiving etanercept or infliximab are at increased risk for serious infections. Expect anakinra to be stopped if serious infection develops.

Be aware that live-virus vaccines shouldn’t be given to patients receiving anakinra because drug decreases immune response.

Monitor patients with impaired renal function for signs of anakinra toxicity; they’re at increased risk because drug is excreted primarily by the kidneys.

Store anakinra at 2° to 8° C (36° to 46° F). Protect from freezing and light.

PATIENT SAFTY

Teach proper injection technique if patient will self-administer drug. Make sure patient understands the process and can correctly prepare and inject doses.

Instruct patient to rotate injection sites among thighs, stomach, and upper arms and to avoid areas that are tender, hard, red, or bruised. Advise him to make sure that each injection site is at least 1 inch away from the previous site.

Urge patient to discard used needles and syringes in a puncture-resistant container and not to reuse them. Instruct him to return container to prescriber for disposal.

Review evidence of allergic reaction, including rash and shortness of breath.

Urge patient to immediately report signs of infection, such as cough, fever, chills, dyspnea, or headache, to prescriber.

Category

Chemical class: Nonsteroidal selective aromatase inhibitor
Therapeutic class: Antineoplastic

Pregnancy category: D

Indications

To treat postmenopausal women with unknown or positive hormone receptor and locally advanced or metastatic breast cancer, and those with advanced breast cancer that progresses after tamoxifen therapy; as adjunct to treat early breast cancer in postmenopausal women with positive hormone receptor Adult women. 1 mg daily.

Contraindications

Hypersensitivity to anastrozole or its components, pregnancy, premenopausal women

Side Efect

CNS: Asthenia, depression, dizziness, headache, hypertonia, insomnia, lethargy, paresthesia
CV: Angina, MI
EENT: Dry mouth, pharyngitis
ENDO: Hot flashes, weight gain
CV: Chest pain, hypertension, peripheral edema, thromboembolic disease, vasodilation
GI: Abdominal or pelvic pain, anorexia, increased appetite, constipation, diarrhea, nausea, vomiting
GU: Leukorrhea; vaginal bleeding, dryness, or hemorrhage
MS: Back or bone pain
RESP: Increased cough, dyspnea
SKIN: Diaphoresis, rash, urticaria
Other: Anaphylaxis, angioedema, flulike symptoms, pain, tumor flare

Cautions

Assess patient for evidence of thromboembolic events during anastrozole therapy, such as shortness of breath, leg pain, and altered mental status.

Assess patient for evidence of ischemic cardiovascular disorders, such as angina and MI, especially in women with ischemic heart disease.

Store drug in a tightly closed container at room temperature.

PATIENT SAFTY

Urge patient to report menopausal status accurately because drug is contraindicated and ineffective in premenopausal women.

Inform patient about possible dizziness and lethargy, and advise her to avoid potentially hazardous activities until drug’s CNS effects are known.

Urge patient to tell prescriber about leg pain or calf swelling, which may indicate a blood clot.

Advise patient to consume adequate calcium and to follow an exercise program; drug may reduce bone mineral density.

Urge patient taking anastrozole to comply with follow-up appointments.

Category

Chemical class: Indanedione derivative
Therapeutic class: Anticoagulant

Pregnancy category: X

Indications

To prevent and treat venous thrombosis, atrial fibrillation with embolization, and pulmonary embolism; as adjunct to treat coronary artery occlusion, usually in patients who can’t tolerate coumarin anticoagulants
Adults. Initial: 300 mg on day 1; then 200 mg on day 2, and 100 mg on day 3. Maintenance: 25 to 250 mg daily. Route Onset Peak Duration P.O. In 6 hr 48–72 hr 1–3 days

Mechanism of Action

Interferes with the liver’s ability to synthesize vitamin K–dependent clotting factors, which results in the depletion of clotting factors II (prothrombin),VII, IX, and X. By depleting levels of vitamin K–dependent clotting factors that are needed to form a stable fibrin clot, anisindione interferes with the clotting cascade and prevents coagulation.

Contraindications

Ascorbic acid deficiency; blood dyscrasias; continuous small-intestine drainage tube; diverticulitis; emaciation; GI, GU, or respiratory tract bleeding; hemophilia; hemorrhagic tendency; history of warfarininduced necrosis; hypersensitivity to anisindione or its components; leukemia; major recent surgery; malnutrition; pericardial effusion; pericarditis; polyarthritis; pregnancy; prostatectomy; recent spinal puncture, percutaneous invasive procedure, diagnostic testing, or insertion of intrauterine device; recent or possible CNS or eye surgery; severe renal or hepatic disease; severe uncontrolled diabetes; severe uncontrolled malignant hypertension; subacute bacterial endocarditis; thrombocytopenic pur-pura; visceral carcinomas; ulcerative colitis

Interactions

abciximab, acetaminophen, allopurinol, alteplase, amiodarone, amitriptyline, amoxapine, androgens, aspirin, beta blockers, cephalosporins, chloral hydrate, Androstenedione Estrone Estradiol Estradiol Estrogen receptor Nucleus Estrogen receptor Nucleus Breast cancer cell Breast cancer cell Aromatase Androstenedione Estrone Estradiol Aromatase Anastrozole Androstenedione Estrone Estradiol Estradiol Estrogen receptor Nucleus Estrogen receptor Nucleus Breast cancer cell Breast cancer cell Aromatase Androstenedione Estrone Estradiol Aromatase Anastrozole

Mechanism of Action

Anastrozole treats certain breast cancers in postmenopausal women by inhibiting the enzyme aromatase, as shown in the illustrations below, thus preventing production of estrone and estradiol. This is how, in women with breast tumors that contain estrogen receptors, anastrozole prevents the stimulatory effects of estrogen on tumor growth. phenicol, chlorpropamide, cimetidine, cisapride, clofibrate, clomipramine, corticosteroids, co-trimoxazole, cyclophosphamide, danazol, desipramine, dextrothyroxine, diclofenac, diflunisal, disulfiram, doxepin, erythromycin, etodolac, fluconazole, fluoxymesterone, fosphenytoin, gemfibrozil, glucagon, hydantoins, ifosfamide, influenza virus vaccines, imipramine, indomethacin, isoniazid, itraconazole, ketoconazole, ketolorac, lepirudin, loop diuretics, lovastatin, low–molecular-weight heparins, meclofenamate, mefenamic acid, methyltestosterone, metronidazole, miconazole, moricizine, nabumetone, naproxen, nalidixic acid, neomycin, nortriptyline, NSAIDs, omeprazole, oxandrolone, penicillins, phenylbutazones, phenytoin, piroxicam, propafenone, propoxyphene, protriptyline, quinidine, quinine, quinolones, reteplase, salicylates, stanazolol, streptokinase, sulfamethoxazole, sulfinpyrazone, sulindac, tamoxifen, testosterone, thioamines, thyroid hormones, tomentin, urokinase: Increased anticoagulant effects aminoglutethimide, ascorbic acid, barbiturates, carbamazepine, cholestyramine, corticosteroids, dicloxacillin, estrogen, ethanol, ethchlorvynol, etretinate, glutethimide, griseofulvin, nafcillin, oral contraceptives, rifampin, spironolactone, sucralfate, thiazide diuretics, thiopurines, trazodone, vitamin K: Decreased anticoagulant effects aminoglycosides, mineral oil, tetracycline, vitamin E: Interference with vitamin K, leading to increased anticoagulant effects enteral products and high in vitamin K, such as dark green leafy vegetables: Interference with anticoagulant effects
alcohol use: Possibly increased or decreased anticoagulation

Side Efect

CNS: Fever, headache
EENT: Blurred vision, mouth ulcers, pharyngitis
GI: Abdominal cramps, diarrhea, hepatic dysfunction, hepatitis, nausea, steatorrhea
GU: Albuminuria, anuria, priaprism, redorange urine, renal tubular necrosis
HEME: Agranulocytosis, anemia, atypical mononuclear cells, eosinophilia, hemorrhage, leukocytosis, leukopenia, RBC aplasia, thrombocytopenia
SKIN: Alopecia, exfoliative dermatitis, jaundice, necrosis of the skin and tissues evidenced by gangrene and purple toes, urticaria

Cautions

Watch for PT to become prolonged 6 hours after anisindione administration, although maximum therapeutic effects may take 48 to 72 hours to appear.
WARNING Watch for signs of overanticoagulation, such as microscopic hematuria, excessive menstrual bleeding, melena, petechiae, and bleeding from superficial trauma, such as tooth brushing or shaving.

Monitor INR, CBC, fecal occult blood test, and urinalysis results for signs of overanticoagulation.

PATIENT SAFTY

Advise patient to avoid alcohol, salicylates, and drastic changes in his intake of vitamin K–rich food.

Instruct patient to promptly report pregnancy to prescriber.

Provide patient with a list of rich in vitamin K. Advise him to eat consistent daily amounts of vitamin K.

Urge patient to consult prescriber before having dental work or elective surgery.

Tell patient to immediately report unusual bleeding, bruising, red or red-orange urine, red or tarry black stools, diarrhea, bleeding from gums or nose, or excessive bleeding from minor cuts or scratches.

Category

Chemical class: p-Anisoylated derivative of the Lys-plasminogen-streptokinase activator complex
Therapeutic class: Thrombolytic enzyme

Pregnancy category: C

Indications

To treat acute MI, lyse thrombi that are anistreplase 88 obstructing coronary arteries, reduce infarct size, improve ventricular function after acute MI, reduce mortality from acute MI

IV

Adults. 30 units injected over 2 to 5 min. Route Onset Peak Duration I.V. Immediate 20 min– 4–6 hr 2 hr

Mechanism of Action

Indirectly promotes conversion of plasminogen to plasmin, an enzyme that breaks down fibrin clots, fibrinogen, and other plasma proteins, including procoagulant factors V and VIII.

Incompatibilities

Don’t add other to anistreplase solution or infuse other through same I.V. line.

Contraindications

Active internal bleeding, arteriovenous malformation or aneurysm, bleeding diathesis, history of stroke, hypersensitivity to anistreplase or streptokinase, intracranial neoplasm, intracranial or intraspinal surgery or trauma within past 2 months, severe uncontrolled hypertension

Interactions

aspirin, dipyridamole, and other that alter platelet function; heparin; vitamin K antagonists: Possibly increased risk of bleeding if administered before anistreplase

Side Efect

CNS: Dizziness, fever, headache, intracranial hemorrhage
CV: Ankle edema, arrhythmias (especially accelerated idioventricular rhythm, conduction disorders, premature ventricular beats, sinus bradycardia, ventricular fibrillation, ventricular tachycardia), hypotension, vasculitis
EENT: Epistaxis
GI: Abdominal pain or swelling, constipation, GI bleeding, nausea, vomiting
GU: Hematuria,proteinuria,vaginal bleeding
HEME: Bleeding tendency, eosinophilia, mild to severe hemorrhage
MS: Arthralgia, back pain, joint stiffness, myalgia
RESP: Bronchospasm, dyspnea, hemoptysis
SKIN: Flushing, pruritus, rash, urticaria
Other: Anaphylaxis (rare), angioedema

Cautions

Use anistreplase cautiously in patients with acute pericarditis; cerebrovascular disease; hemorrhagic ophthalmic conditions; history of major surgery, GI or GU bleeding, or trauma within past 10 days; hypertension; mitral stenosis with atrial fibrillation; pregnancy; septic thrombophlebitis; severe hepatic or renal disease; or subacute bacterial endocarditis.

Reconstitute anistreplase by slowly directing 5 ml of sterile water for injection USP or sodium chloride for injection against side of vial. Then gently roll vial to mix dry powder and fluid and minimize foaming. Don’t shake vial. The resulting solution should be colorless to pale yellow and transparent.

Before administering, inspect solution for particles and discoloration. If present, discard and reconstitute drug from a new vial. Then withdraw entire contents of vial. Don’t dilute reconstituted solution further or add it to I.V. fluid. Don’t add other to vial or syringe that contains anistreplase. Discard drug if not given within 30 minutes after reconstitution.

For maximum effectiveness, expect to administer anistreplase as soon as possible after onset of MI symptoms.

Closely monitor all puncture sites, such as catheter insertion and needle puncture sites, for bleeding.

Don’t give I.M. injections, and avoid handling patient unnecessarily during anistreplase therapy. Perform venipuncture only when necessary.

If an arterial puncture is needed after anistreplase administration, use an arm vessel that allows easy manual compression. Apply a pressure dressing afterward, and check puncture site often for bleeding.

Use continuous cardiac monitoring because arrhythmias may occur during reperfusion. Keep antiarrhythmics on hand during anistreplase therapy, and manage arrhythmias using facility policy.

Keep epinephrine nearby for anaphylaxis.

Know that anistreplase may be less effective if given more than 5 days after anistreplase or streptokinase administration. This occurs because patient may have developed antistreptokinase antibodies, which makes him more resistant to the drug and drug therapy less effective. Elevated serum antistreptokinase antibody levels and reduced drug effectiveness can persist for 5 days to 12 months.

Closely monitor blood coagulation test results. The drug markedly decreases plasminogen and fibrinogen levels and increases thrombin time, APTT, and PT.

PATIENT SAFTY

Instruct patient to report

Side Efect

immediately, especially bleeding, dizziness, and chest pain.

Category

Chemical class: Recombinant protein
Therapeutic class: Antihemophilic factor

Pregnancy category: C

Indications

To prevent and control bleeding episodes in patients with hemophilia A and factor VIII inhibitors not exceeding 10 Bethesda Units/ml I.V. INJECTION Adults and children. Highly individualized. For early hemarthrosis, muscle bleeding episode, or mild oral bleeding episode: Dose given to achieve peak post-infusion factor VIII activity in blood (determined by multiplying dose given/kg body weight by 2) 20% to 40% of normal with infusions every 12 to 24 hr for 1 to 3 days until bleeding episode resolved. For more extensive hemarthrosis, muscle bleeding episode, or hematoma: Dose given to achieve peak post-infusion factor VIII activity in blood 30% to 60% of normal with infusions every 12 to 24 hr for 3 or more days until pain and disability are resolved. For life-threatening bleeding episodes: Dose given to achieve peak postinfusion factor VIII activity in blood 60% to 100% with infusions every 8 to 24 hr until bleeding episode stops. To prevent and control perioperative bleeding in patients with hemophilia A I.V. INJECTION Adults and children. Highly individualized. For minor surgery, including tooth extraction: Dose given to achieve peak postinfusion factor VIII activity in blood (determined by multiplying dose given/kg body weight by 2) between 60% and 100% of normal, given as a single bolus infusion within 1 hr of operation, with optional additional dose every 12 to 24 hr, as needed. For major surgery: Dose given to achieve peak postinfusion factor VIII activity in blood 80% to 100% before and after surgery with infusions every 8 to 24 hr.
I.V.INJECTION(KOGENATE FS) Adults and children. Highly individualized based on this formula: Body weight (kg) 3 desired factor VIII rise (international units/dL or % of normal) 3 0.5 (international units/kg per international units/dL). For minor surgery, including tooth extraction: 15 to 30 international units/kg to achieve desired factor VIII rise to 30% to 60% of normal with injections repeated every 12 to 24 hr until bleeding has resolved. For major surgery: 50 international units/kg preoperatively to achieve a desired factor VIII rise to 100% of normal with dosage repeated 6 to 12 hr after initial dose as needed, and for 10 to 14 days thereafter, as needed, until healing is complete.
IV:(XYNTHA) antihemophilic factor 90 Adults and children.Highly individualized based on this formula: Body weight (kg) 3 desired factor VIII rise (international units/dL or % of normal) 3 0.5 (international units/kg per international units/dL). For minor surgery, including tooth extraction: Desired factor VIII rise is 30% to 60% of normal with infusions every 12 to 24 hr for 3 to 4 days or until adequate local hemostasis is achieved (for tooth extraction, a single infusion plus oral antifibrinolytic therapy within 1 hr may be sufficient). For major surgery: Desired factor VIII rise is 60% to 100% of normal with infusions every 8 to 24 hr until adequate local hemostasis and wound healing are achieved. To prevent or treat bleeding in hemophilia A I.V. INJECTION (HUMATE-P)
Adults. Highly individualized. For mild hemorrhage, such as early joint or muscle bleed or severe epistaxis: Loading dose of 15 international units/kg to achieve factor VIII:C plasma level about 30% of normal, with half the loading dose repeated once or twice daily for 1 to 2 days as needed. For moderate hemorrhage, such as advanced joint or muscle bleed; neck, tongue, or pharyngeal hematoma without airway compromise; tooth extraction; or severe abdominal pain: Loading dose of 25 international units/kg to achieve factor VIII:C plasma level about 50% of normal, followed by 15 international units/kg every 8 to 12 hr for first 1 to 2 days to maintain factor VIII:C plasma level at 30% of normal, and then 15 international units/kg once or twice daily for total of up to 7 days or until adequate wound healing. For life-threatening hemorrhage, as may occur in major surgery; GI bleeding; neck, tongue, or pharyngeal hematoma with potential for airway compromise; intracranial, intra-abdominal, or intrathoracic bleeding; or fractures: Loading dose of 40 to 50 international units/kg, followed by 20 to 25 international units/kg every 8 hr to maintain factor VIII:C plasma level at 80% to 100% of normal for 7 days, followed by 20 to 25 international units/kg once or twice daily for another 7 days to maintain factor VIII:C level at 30% to 50% of normal.
I.V.INJECTION(KOGENATE FS) Adults and children.Highly individualized based on this formula: Body weight (kg) 3 desired factor VIII rise (international units/dL or % of normal) 3 0.5 (international units/kg per international units/dL). For early hemarthrosis or minor muscle or oral bleeds: 10 to 20 international units/kg to achieve desired factor VIII rise of 20% to 40% of normal, dosage repeated, if needed. For moderate bleeding into muscles, mild head trauma, or bleeding into oral cavity: 15 to 30 international units/kg to achieve desired factor VIII rise of 30% to 60% of normal with injections every 12 to 24 hr until bleeding has resolved. For major GI bleeding; intracranial, intra-abdominal or intrathoracic bleeding; or fractures: Initial dose of 40 to 50 international units/kg followed by repeat dose of 20 to 25 international units/kg to achieve desired factor VIII rise of 60% to 100% of normal with injections of 20 to 25 international units/kg repeated every 8 to 24 hr until bleeding has resolved.
IV:(XYNTHA) Adults and children.Highly individualized based on this formula: Body weight (kg) 3 desired factor VIII rise (international units/dL or % of normal) 3 0.5 (international units/kg per international units/dL). For early hemarthrosis or minor muscle or oral bleeds: Desired factor VIII rise is 20% to 40% of normal with infusions every 12 to 24 hr for at least 1 day, depending on the severity of the bleeding episode. For moderate bleeding into muscles, mild head trauma, or bleeding into the oral cavity: Desired factor VIII rise is 30% to 60% of normal with infusions every 12 to 24 hr for 3 to 4 days or until adequate local hemostasis is achieved. For major GI bleeding; intracranial, intra-abdominal, or intrathoracic bleeding; or fractures: Desired factor VIII rise is 60% to 100% of normal with infusions every 8 to 24 hr until bleeding has resolved. To treat spontaneous and traumainduced bleeding episodes and prevent excessive bleeding during and after surgery in patients with von Willebrand disease when use of desmopressin is inadequate I.V. INJECTION (HUMATE-P) Adults and children. 40 to 80 international units/kg every 8 to 12 hr as needed. To prevent excessive bleeding during and after surgery in patients with von Willebrand disease I.V. INJECTION (HUMATE-P) Adults and children. Highly individualized. For emergency surgery: Loading dose of 50 to 60 international uits/kg, followed by half the loading dose every 6 to 12 hr as needed. For preplanned surgery: Individualized loading dose based on patient need 1 to 2 hr before surgery, followed by half the loading dose every 6 to 12 hr for at least 12 hr (oral surgery), 48 hr (minor surgery), or 72 hr (major surgery). Route Onset Peak Duration I.V. Immediate 5 min Unknown

Mechanism of Action

Provides supplemental factor VIII, the coagulation factor required for blood to clot that’s missing in patients with hemophilia A and diminished in patients with factor VIII inhibitors. After blood clots, bleeding stops.

Contraindications

Life-threatening, immediate hypersensitivity reactions, including anaphylaxis, experienced with prior administration of drug or exposure to mouse or hamster proteins

Side Efect

CNS: Dizziness, fever, headache, rigidity
CV: Chest pain, hypotension
EENT: Taste perversion
ENDO: Hot flashes
GI: Abdominal pain, diarrhea, nausea, vomiting
HEME: Bleeding tendency, decreased coagulation factor VIII, decreased hematocrit, hematoma, hemolytic anemia
MS: Joint swelling, lower limb edema
RESP: Dyspnea, shortness of breath
SKIN: Diaphoresis, pruritus, rash, urticaria
Other: Anaphylaxis, angioedema, catheterrelated infection, injection site reactions

Cautions

Check to confirm that clotting defect is factor VIII deficiency (Kogenate FS or Xyntha only) or von Willebrand disease (Humate-P only) before giving antihemophilic factor (recombinant) because drug isn’t effective in treating other coagulation factor deficiencies.

Reconstitute Advate or Alphanate using sterile water for injection. Bring both drug and diluent to room temperature; then clean stoppers with antiseptic solution and let dry. Remove protective covering from one end of double-ended needle and insert through center of diluent stopper. Remove protective covering from other end of double-ended needle. Invert diluent bottle over upright drug bottle; then rapidly insert free end of needle through drug stopper at center. The vacuum in bottle will draw in the diluent. Then disconnect the two bottles by removing needle from diluent bottle stopper, and remove the needle from drug bottle. Swirl gently until all drug is dissolved. Avoid shaking to prevent foaming and degradation of drug. Administer in a separate line within 3 hours of reconstitution.

Reconstitute Humate-P, Kogenate FS, and Xyntha according to manufacturer instructions in package insert.

Take patient’s pulse before and periodically during drug administration. If pulse rate increases significantly, reduce administration rate or temporarily halt injection to let pulse rate return to preadministration level before resuming administration.

To administer Advate or Alphanate, use only plastic material because protein in drug will adhere to glass. Attach filter needle to syringe and draw back plunger to draw air into syringe. Insert needle into reconstituted drug vial. Inject air into bottle and then withdraw drug from vial. Remove and discard filter needle from syringe, attach a suitable needle, and inject I.V. bolus at no more than 10 ml/min over no more than 5 minutes.

To give Humate-P, slowly inject I.V. bolus at no more than 4 ml/min using a venipuncture or other suitable I.V. injection set.

To give Kogenate FS, check patient’s pulse; then slowly inject intravenously over 1 to 15 minutes, checking pulse rate throughout administration. If pulse rises significantly, slow administration or temporarily stop delivery to let pulse rate to return to normal; then continue administration.

To administer Xyntha, slowly infuse intravenously over several minutes at a rate comfortable for the patient. Don’t infuse antihemophilic factor 92 in tubing or container that contains other .

Monitor patient’s plasma factor VIII levels (and von Willebrand factor: Ristocetin cofactor if patient has von Willebrand disease) during and after treatment to ensure adequate levels have been reached and are being maintained, as ordered.

Monitor patient for anaphylaxis, and have emergency equipment nearby.

After giving drug, monitor patient for formation of neutralizing antibodies to factor VIII, a known complication in hemophilia A treatment that may cause continued bleeding. Obtain laboratory analysis to detect neutralizing antibodies, as ordered.

Watch for hemolysis when giving large doses to patients with blood types A, B, and AB.

PATIENT SAFTY

Teach patient and caregivers how to administer antihemophilic factor (recombinant) at home in an emergency.

Explain that drug may be stored in the refrigerator or at room temperature but that it shouldn’t be exposed to temperatures above 77° F (25° C) or below freezing because they may alter effectiveness.

Instruct patient to stop drug and seek emergency help immediately if he has an acute allergic reaction, such as hives, chest tightness, wheezing, low blood pressure, or fainting, during or after administration.

Category

Chemical class: Alpha2-globulin
Therapeutic class: Anticoagulant, antithrombotic

Pregnancy category: C

Indications

To treat patients with hereditary antithrombin III (AT-III) deficiency who are undergoing surgery or obstetric procedures or who have thromboembolism
I.V.INJECTION Adults and children.Initial: Individualized (based on weight, degree of AT-III deficiency, and desired level of AT-III to be achieved) sufficient to increase AT-III activity to 120% of normal, given at 50 to 100 international units/min. Maintenance: Individualized dosage sufficient to keep AT-III activity at 80% or more of normal, administered every 24 hr, continued for 2 to 8 days, depending on the patient’s condition and history and prescriber’s judgment. A pregnant, immobilized, or postsurgical patient may need more prolonged therapy. Route Onset Peak Duration I.V. Immediate Unknown 4 days

Mechanism of Action

Inhibits blood coagulation by inactivating thrombin; activated forms of factors IX, X, XI, and XII; and plasmin.

Interactions

heparin: Enhanced anticoagulant effect

Side Efect

CNS: Chills, dizziness, fever, light-headedness
CV: Chest pain or tightness, hypotension, vasodilation
EENT: Unpleasant taste
GI: Abdominal cramps, bowel fullness, nausea
GU: Diuresis
HEME: Hematoma
RESP: Dyspnea
SKIN: Oozing lesions, urticaria

Cautions

Reconstitute AT-III with 10 ml sterile water for injection (provided by manufacturer) or alternate solution, such as normal saline solution or D5W injection. Don’t shake vial during reconstitution. Let solution come to room temperature before administration. If desired, dilute reconstituted solution further, using same diluent.
WARNING Don’t use diluent that contains benzyl alcohol to reconstitute drug for a neonate. It can cause a fatal toxic syndrome with metabolic acidosis, CNS depression, respiratory problems, renal failure, hypotension, seizures, and antithrombin III,intracranial hemorrhage.

Don’t refrigerate reconstituted solution. Use within 3 hours; discard unused portion.

Administer AT-III alone. Don’t mix it with other or solutions.

If after 30 minutes the initial dose doesn’t increase AT-III activity to 120% of normal, expect prescriber to increase dosage.

If patient requires a dosage increase, monitor AT-III activity more often and expect to adjust dosage accordingly.

To avoid bleeding, anticipate a reduction in heparin dosage during AT-III therapy.

If mild

Side Efect

occur, decrease infusion rate, as prescribed. If severe reactions occur, discontinue infusion, as prescribed, until they subside.

Evaluate serum AT-III level twice daily until dosage is stabilized. After that, evaluate level once daily, just before a dose.

PATIENT SAFTY

Tell patient that blood will be drawn periodically to guide

Category

Chemical class: Nonergoline dopamine agonist
Therapeutic class: Hypomobilic antiparkinsonian

Pregnancy category: C

Indications

To treat hypomobility “off” episodes (end-of-dose wearing off and unpredictable on/off episodes) in advanced Parkinson’s disease SUBCUTANEOUS INJECTION
Adults. Initial: 0.2 ml (2 mg) p.r.n. adjusted as needed in 0.1-ml (1-mg) increments every few days. Maximum: 0.6 ml (6 mg).
DOSAGE ADJUSTMENT For patients who tolerate 0.2 ml (2 mg) but have no response, a 0.4-ml (4-mg) dose may be given under medical supervision, with standing and supine blood pressure checked every 20 min for 1 hr at the next observed “off”period, as long as it is at least 2 hr after the initial 0.2-ml (2-mg) test dose. If tolerated, a dose 0.1 ml (1 mg) lower may be given p.r.n. and increased in 0.1-ml (1-mg) increments every few days as needed to a maximum dose of 0.6 ml (6 mg). If patient doesn’t tolerate a 0.4-ml (4-mg) test dose, a 0.3-ml (3-mg) test dose may be given under medical supervision, with standing and supine blood pressure checked every 20 min for 1 hr at the next observed “off”period, as long as it is at least 2 hr after the initial 0.4-ml (4-mg) test dose. If tolerated, a 0.2-ml (2-mg) dose can be started p.r.n. and increased to no more than 0.3 ml (3 mg) if needed after a few days. For patients with mild to moderate renal impairment, the initial dose should be reduced to 0.1 ml (1 mg). Route Onset Peak Duration SubQ 10–60 min Unknown Unknown

Mechanism of Action

May stimulate postsynaptic dopamine D2 receptors in the caudate-putamen of the brain. As a result, apomorphine improves motor function and activity levels in patients with Parkinson’s disease.

Contraindications

Concurrent use of 5-HT3antagonists, such as alosetron, dolasetron, granisetron, ondansetron, and palonosetron; hypersensitivity to apomorphine or its components, including sodium metabisulfite

Interactions

5-HT3antagonists: Increased risk of profound hypotension and loss of consciousness antihypertensives, vasodilators: Increased risk of serious

Side Efect

, such as hypotension, MI, and bone or joint injuries dopamine antagonists (such as butyrophenones, metoclopramide, phenothiazines, thioxanthenes): Decreased apomorphine effectiveness that prolong QT interval: Increased risk of torsades de pointes entacapone, tolcapone: Increased risk of tachycardia, hypertension, and arrhythmias
alcohol use: Increased risk of hypotension apomorphine hydrochloride 94

Side Efect

CNS: Aggravated Parkinson’s disease, anxiety, confusion, depression, dizziness, drowsiness, dyskinesia, euphoria, fatigue, hallucinations, headache, insomnia, somnolence, weakness, yawning
CV: Angina, chest pain, congestive heart failure, edema, MI, orthostatic hypotension, prolonged QT interval
EENT: Rhinorrhea
GI: Constipation, diarrhea, nausea, vomiting
GU: UTI
MS: Arthralgia, back or limb pain
RESP: Dyspnea, pneumonia, tachypnea
SKIN: Contact dermatitis, diaphoresis, ecchymosis, flushing, pallor
Other: Dehydration; injection site bruising, granuloma, or pruritus; intense urges to perform certain activities, such as gambling and sexual acts

Cautions

Use apomorphine cautiously in patients with hepatic or renal insufficiency.

An antiemetic, such as trimethobenzamide 300 mg t.i.d., should be started 3 days before apomorphine starts and continue for at least the first 2 months of therapy. Apomorphine may cause severe nausea and vomiting, even with an antiemetic.

Monitor patient’s blood pressure closely because drug can cause severe orthostatic hypotension.

Give a 0.2-ml (2-mg) test dose of apomorphine, as prescribed, and then check patient’s supine and standing blood pressure 20, 40, and 60 minutes later.

Monitor patient closely if he has an increased risk of prolonged QT interval, as from hypokalemia, hypomagnesemia, bradycardia, use of certain , or genetic predisposition. QT-interval prolongation may lead to torsades de pointes.

Monitor patient for evidence of apomorphine abuse. Although rare, drug may cause psychosexual stimulation and increased libido, which may cause patient to use it more often than needed for reducing Parkinson’s disease symptoms.

Assess patient regularly for skin changes because melanoma risk is higher in those with Parkinson’s disease. It isn’t clear whether the risk is increased by the disease or by its treatment.

PATIENT SAFTY

Explain that an antiemetic will be prescribed starting 3 days before first apomorphine dose. Urge patient to take the antiemetic exactly as prescribed. Explain that it will be needed for 2 months or longer during apomorphine therapy.

Explain that a test dose will determine response and drug’s effects on blood pressure before patient goes home with drug.

Teach patient how to use dosing pen and how to give drug subcutaneously.

Emphasize that apomorphine doses are expressed as milliliters, not milligrams. Tell patient to draw up each dose carefully to reduce the chance of dosage error.

Instruct patient to rotate injection sites in a systematic manner.

Stress importance of taking apomorphine only as prescribed because serious adverse reactions may occur.

Advise patient to avoid hazardous activities until drug’s CNS effects are known. In particular, caution patient that apomorphine increases the risk of falling asleep suddenly, without feeling sleepy.

Urge patient to have regular skin examinations by a dermatologist or other qualified health professional.

Instruct patient to notify prescriber about intense urges, such as for gambling or sex, because dosage may need to be reduced or drug discontinued.

Category

Chemical class: Substance P/neurokinin 1 (NK1) receptor antagonist
Therapeutic class: Antiemetic

Pregnancy category: B

Indications

To prevent acute and delayed nausea and vomiting associated with highly emetogenic chemotherapy, including high-dose
Adults. 125 mg 1 hr before chemotherapy treatment, followed by 80 mg daily in morning on next 2 days.
IV:
Adults. 115 mg 30 min before chemotherapy begins (day 1 only). To prevent postoperative nausea and vomiting
Adults. 40 mg within 3 hr before induction of anesthesia Route Onset Peak Duration P.O., I.V. Unknown 4 hr Unknown

Mechanism of Action

Crosses the blood–brain barrier to occupy brain NK1 receptors, which prevents nerve transmission of signals that cause nausea and vomiting.

Contraindications

Hypersensitivity to aprepitant, polysorbate 80, or their components; use of astemizole, cisapride, pimozide, or terfenadine

Interactions

carbamazepine, phenytoin,
rifampin: Possibly decreased blood aprepitant level corticosteroids: Increased blood corticosteroid level CYP2C9 metabolizers (such as phenytoin, tolbutamide, and warfarin): Decreased blood level and effectiveness of CYP2C9 metabolizers CYP3A4 inhibitors (such as clarithromycin, diltiazem, itraconazole, ketoconazole, nefazodone, nelfinavir, and troleandomycin): Increased blood aprepitant level CYP3A4 substrates (such as astemizole, benzodiazepines, cisapride, docetaxel, etoposide, ifosfamide, imatinib, irinotecan, paclitaxel, pimozide, terfenadine, vinblastine, vincristine, and vinorelbine): Increased level of CYP3A4 substrates, resulting in possibly serious or life-threatening

Side Efect

oral contraceptives: Possibly decreased effectiveness of oral contraceptives paroxetine: Possibly decreased blood level of both

Side Efect

CNS: Anxiety, asthenia, confusion, depression, dizziness, fatigue, fever, headache, insomnia, malaise, peripheral or sensory neuropathy, somnolence
CV: Deep vein thrombosis, edema, hypertension, hypotension, tachycardia
EENT: Increased salivation, mucous membrane alteration, nasal discharge, pharyngitis, stomatitis, taste perversion, tinnitus, vocal disturbance
ENDO: Hot flashes, hyperglycemia
GI: Abdominal pain, anorexia, constipation, diarrhea, dysphagia, elevated liver function test results, epigastric discomfort, flatulence, gastritis, gastroesophageal reflux, heartburn, hiccups, nausea, obstipation, vomiting
GU: Dysuria, elevated BUN and serum creatinine levels, hematuria, leukocyturia, renal insufficiency
HEME: Anemia, febrile neutropenia, leukocytosis, thrombocytopenia
MS: Muscle weakness, myalgia, pelvic pain
RESP: Cough, dyspnea, non–small-cell lung carcinoma, pneumonitis, pulmonary embolism, respiratory insufficiency, respiratory tract infection
SKIN: Alopecia, diaphoresis, flushing, pruritus, rash, urticaria
Other: Anaphylaxis, angioedema, dehydration, hypokalemia, hyponatremia, infusion site pain or induration, malignant neoplasm, septic shock, weight loss

Cautions

Use caution when giving aprepitant to patients with severe hepatic insufficiency because drug’s effects on such patients aren’t known.

For maximum antiemetic effects, expect to administer aprepitant with dexamethasone and a 5-HT3antagonist, such as dolasetron, granisetron, or ondansetron.

Drug is given intravenously only as the first dose 30 minutes before chemotherapy. Later doses are given orally.

To reconstitute parental aprepitant, inject 5 ml normal saline for injection along vial wall to prevent foaming. Swirl vial gently. Withdraw contents from vial and add to an infusion bag containing 110 ml normal saline solution. Gently invert the bag two or three times. Administer over 15 minutes. Reconstituted solution may be stored at room temperature for 24 hours. aprepitant 96

PATIENT SAFTY

Instruct patient to take 125-mg dose of oral aprepitant 1 hour before chemotherapy, 80-mg dose in the morning for 2 days after chemotherapy, or 40-mg dose within 3 hours before induction of anesthesia.

Tell female patients taking oral contraceptives to use an alternative or backup method of contraception during aprepitant therapy and for 1 month after last dose because drug reduces effectiveness of oral contraceptives.

Tell patient taking warfarin to have clotting status monitored closely for 2 weeks after first aprepitant dose, especially every 7 to 10 days during each chemotherapy cycle in which the drug is used.

Caution patient to inform prescriber of any he’s taking, including OTC and herbal preparations, because they may interact with aprepitant.

Category

Chemical class: Selective beta2-adrenergic agonist, sympathomimetic
Therapeutic class: Bronchodilator

Pregnancy category: C

Indications

To provide maintenance treatment of bronchoconstriction in patients with COPD, including chronic bronchitis and emphysema INHALATION SOLUTION
Adults.15 mcg (contents of one 2-ml vial) b.i.d. (morning and evening) via nebulization. Do not exceed 30 mcg daily.

Mechanism of Action

Attaches to beta2receptors on bronchial cell membranes, stimulating the intracellular enzyme adenylate cyclase to convert adenosine triphosphate to cyclic adenosine monophosphate (cAMP). The resulting increase in intracellular cAMP level relaxes bronchial smooth-muscle cells, stabilizes mast cells, and inhibits histamine release.

Contraindications

Hypersensitivity to arformoterol, racemic formoterol, or its components; acute bronchospasm; symptoms of COPD

Interactions

beta blockers: Decreased effectiveness of either drug corticosteroids, methylxanthines such as aminophylline or theophylline, non–potassium-sparing (such as loop and thiazide) diuretics: Increased risk of hypokalmia known to prolong the QT interval, MAO inhibitors, tricyclic antidepressants: Increased risk of life-threatening ventricular arrhythmias thyroid hormones: Increased risk of coronary insufficiency

Side Efect

CNS: Agitation, asthenia, circumoral paresthesia, fatigue, fever, headache, hypokinesia, insomnia, malaise, nervousness, paralysis, somnolence, stroke, tremor
CV: Angina, arrhythmias, atrial flutter, chest pain, congestive heart failure, dizziness, heart block, hyperlipemia, hypertension, hypertension, MI, palpitations, peripheral edema, prolonged QT interval
EENT: Abnormal vision, dry mouth, glaucoma, herpes simplex or zoster, oral candidiasis, rectal hemorrhage, sinusitis, voice alteration
ENDO: Hyperglycemia, hypoglycemia
GI: Constipation, diarrhea, gastritis, melena, nausea, pelvic pain, retroperitoneal hemorrhage, vomiting
GU: Cystitis, hematuria, nocturia, PSA elevation, pyuria, renal calculi
HEME: Leukocytosis
MS: Arthralgia, arthritis, back pain, leg or muscle cramps, neck rigidity
RESP: Bronchitis, bronchospasm, COPD, pulmonary congestion
SKIN: Discoloration, dryness, hypertrophy, photosensitivity, rash, urticaria
Other: Anaphylaxis, angioedema, dehyrdation, flulike syndrome, gout, hyperkalemia, hypokalemia, metabolic acidosis

Cautions

Use cautiously in patients with cardiovascular disorders, especially insufficiency, cardiac arrhythmias, and hypertension; convulsive disorders; thyrotoxicosis; and unusual sensitivity to sympathomimetic amines because arformoterol may cause significant adverse effects.

Arformoterol shouldn’t be used to relieve bronchospasm quickly because of its prolonged onset of action. Patients already taking the drug twice daily shouldn’t take additional doses for exercise-induced bronchospasm.

Arformoterol shouldn’t be used with other inhaled, long-acting beta2-agonists or with other medications containing long-acting beta2-agonists.
WARNING Asthma-related deaths may increase in patients receiving salmeterol, a drug in the same class as arformoterol. Monitor patient closely, and notify prescriber immediately of any changes in patient’s respiratory status.

Watch for arrhythmias and changes in heart rate or blood pressure after use in patients with cardiovascular disorders because of drug’s beta-adrengeric effects.
WARNING Stop arformoterol immediately and notify prescriber if patient develops paradoxical bronchospasm or an allergic reaction.

Monitor patient’s blood glucose level, especially if diabetic, and plasma potassium level, as ordered, because arformoterol may cause significant changes.

PATIENT SAFTY

Advise patient to take doses 12 hours apart, morning and evening, for optimum effect. Caution against using drug more than every 12 hours.

Teach patient to self-administer drug with a standard jet nebulizer connected to an air compressor and to use vial immediately after removing from foil package.

Caution patient not to swallow solution.

Tell patient to return unused vials to pouch and store arformoterol in the refrigerator.

Instruct patient taking inhaled, shortacting beta2-agonists on a regular basis to discontinue regular use of these and to use them only for symptomatic relief of acute respiratory symptoms.

Instruct patient to notify prescriber if he needs four or more oral inhalations of rapid-acting inhaled bronchodilator a day for 2 or more consecutive days, or if he uses more than one canister of rapid-acting bronchodilator in an 8-week period.

Category

Chemical class: N2-substituted derivative of arginine
Therapeutic class: Anticoagulant

Pregnancy category: B

Indications

To prevent or treat thrombosis in patients with heparin-induced thrombocytopenia (HIT)
IV:
Adults. 2 mcg/kg/min as a continuous infusion. Maximum: 10 mcg/kg/min.
DOSAGE ADJUSTMENT Dosage adjusted as prescribed to maintain patient’s APTT at 1.5 to 3 times the initial baseline value, not to exceed 100 sec. Initial dosage reduced to 0.5 mcg/kg/min for patients with moderate hepatic impairment. To prevent or treat thrombosis in patients with or at risk for HIT when undergoing percutaneous coronary intervention (PCI)
IV:
Adults. Initial: 350 mcg/kg over 3 to 5 min followed by continuous infusion of 25 mcg/ kg/min.
DOSAGE ADJUSTMENT Dosage adjusted as prescribed to keep activated clotting time (ACT) at 300 to 450 sec. If ACT is less than 300 sec, give additional I.V. bolus dose of 150 mcg/kg and increase infusion to 30 mcg/kg/min; if ACT exceeds 450 sec, reduce dosage to 15 mcg/kg/min. For dissection, impending abrupt closure, thrombus formation during PCI, or inability to reach or keep ACT above 300 sec, give additional bolus dose of 150 mcg/kg and increase infusion to 40 mcg/kg/min. Route Onset Peak Duration I.V. Immediate 3–4 hr Unknown

Mechanism of Action

Forms a tight bond with thrombin, neutralizing this enzyme’s actions, even when the enzyme is trapped within clots. Thrombin causes fibrinogen to convert to fibrin, which is essential for clot formation. argatroban 98

Contraindications

Active major bleeding, hypersensitivity to argatroban or its components

Interactions

alteplase, antineoplastic , antiplatelets, antithymocyte globulin, heparin, NSAIDs, reteplase, salicylates, streptokinase, strontium chloride Sr 89,
warfarin: Increased risk of bleeding porfimer: Possibly decreased efficacy of porfimer photodynamic therapy

Side Efect

CNS: Cerebrovascular bleeding, fever, headache
CV: Atrial fibrillation, cardiac arrest, hypotension, unstable angina, ventricular tachycardia
GI: Abdominal pain, anorexia, diarrhea, elevated liver function test results, GI bleeding, melena, nausea, vomiting
GU: Elevated BUN and serum creatinine levels, hematuria (microscopic), UTI
HEME: Hypoprothrombinemia, unusual bleeding or bruising
RESP: Cough, dyspnea, hemoptysis, pneumonia
SKIN: Bleeding at puncture site, rash
Other: Sepsis

Cautions

WARNING Argatroban isn’t recommended for PCI patients with significant hepatic disease or AST/ALT levels three times or more the upper limits of normal.

Reconstitute drug to 1 mg/ml before giving.

Protect solution from direct sunlight.
WARNING Monitor patients with thrombocytopenia or those receiving daily doses of salicylates greater than 6 g for signs and symptoms of bleeding because they’re at increased risk of bleeding from hypoprothrombinemia.
WARNING Expect to perform blood coagulation tests before and 2 hours after start of therapy because of the major risk of bleeding associated with argatroban. Be aware that coagulopathy must be ruled out before therapy starts. When giving drug to a patient undergoing PCI, expect to check ACT 5 to 10 minutes after each bolus and each infusion rate change and every 20 to 30 minutes during the PCI.

Monitor the following patients for signs and symptoms of bleeding because they’re at increased risk during argatroban therapy: women with active menstruation; patients with vascular or organ abnormalities, such as severe uncontrolled hypertension, advanced renal disease, infective endocarditis, dissecting aortic aneurysm, diverticulitis, hemophilia, hepatic disease (especially if associated with a deficiency of vitamin K–dependent clotting factors), inflammatory bowel disease, or peptic ulcer disease; and those who have recently had a stroke, major surgery (including eye, brain, or spinal cord surgery), large vessel puncture or organ biopsy, lumbar puncture, spinal anesthesia, or major bleeding (including intracranial, GI, intraocular, retroperitoneal, or pulmonary bleeding).

Whenever possible, avoid I.M. injections in patients receiving argatroban to decrease the risk of bleeding.

Thrombin times may not be helpful for monitoring argatroban activity because the drug affects all thrombin-dependent coagulation tests.

Expect dosage to be tapered before stopping to prevent the risk of rebound hypercoagulopathy; drug’s effects last only a short time once drug is discontinued.

PATIENT SAFTY

Inform patient that argatroban is a blood thinner that’s given in the hospital by infusion into a vein. If he needs long-term anticoagulation, he’ll be switched to another drug before discharge.

Advise patient to immediately report unusual or unexplained bleeding, such as blood in urine, easy bruising, nosebleeds, tarry stools, and vaginal bleeding.

Instruct patient to avoid injury while receiving argatroban. For example, suggest that he brush his teeth gently, using a softbristled toothbrush, and take special care when flossing.

Category

Chemical class: Dihydrocarbostyril
Therapeutic class: Atypical antipsychotic

Pregnancy category: C

Indications

To treat acute schizophrenia; to maintain stability in patients with schizophrenia

ORALL

, ORALLY DISINTEGRATING ,
Adults. Initial: 10 or 15 mg daily. Increased to 30 mg daily, as needed, with dosage adjustments at 2-wk intervals. Maintenance: 15 mg daily. To treat acute manic and mixed episodes in bipolar I disorder with or without psychotic features; to maintain stability in patients with bipolar I disorder; as adjunct with lithium or valproate in patients with bipolar I disorder

ORALL

, ORALLY DISINTEGRATING ,
Adults.Initial: 15 mg daily, increased to 30 mg daily, as needed. Maintenance: 15 to 30 mg daily. Maximum: 30 mg daily. Children ages 10 to 17. Initial: 2 mg daily, increased after 2 days to 5 mg daily and then after 2 days to 10 mg daily. Increased in 5-mg increments, as needed, at 2-wk intervals. Maintenance: Lowest dose possible to maintain remission. Maximum: 30 mg daily. As adjunct to treat depression in patients already taking an antidepressant

ORALL

, ORALLY DISINTEGRATING ,
Adults. Initial: 2 to 5 mg daily, with dosage increased to 5 mg daily at 1-wk intervals. To treat agitation in schizophrenia or bipolar mania
I.M.INJECTION
Adults. Initial: Depending on severity of agitation, 5.25 to 15 mg. May be repeated 2 or more hr later, as needed. Maximum: 30 mg daily. To treat irritability associated with autistic disorder

ORALL

, ORALLY DISINTEGRATING , Children. Initial: 2 mg daily, with dosage increased after 1 wk to 5 mg daily and then after 1 wk to 10 mg daily and then after 1 wk to 15 mg daily, as needed.
DOSAGE ADJUSTMENT Dosage reduced to half normal amount when given with clarithromycin, fluoxetine, itraconazole, ketoconazole, paroxetine, or quinidine. Dosage doubled when given with carbamazepine.

Mechanism of Action

May produce antipsychotic effects through partial agonist and antagonist actions. Aripiprazole acts as a partial agonist at dopamine (especially D2) receptors and serotonin (especially 5-HT1A) receptors. The drug acts as an antagonist at 5-HT2A serotonin receptor sites.

Contraindications

Breast-feeding, hypersensitivity to aripiprazole or its components

Interactions

anticholingerics: Increased risk for potentially fatal elevation of body temperature carbamazepine and other CYP3A4 inducers: Possibly increased clearance and decreased blood level of aripiprazole clarithromycin, fluoxetine, paroxetine, quinidine, and other CYP2D6 inhibitors; ketoconazole and other CYP3A4 inhibitors: Possibly inhibited aripiprazole elimination and increased blood level
CNS depressants: Increased CNS depression
alcohol use: Increased CNS depression

Side Efect

CNS: Abnormal gait, agitation, akathisia, anxiety, asthenia, cognitive and motor impairment, confusion, delusions, depression, dizziness, dream disturbances, dystonia, extrapyramidal reactions, fatigue, fever, hallucinations, headache, hostility, insomnia, intracranial hemorrhage, lethargy, light-headedness, mania, nervousness, neuroleptic malignant syndrome, paranoia, restlessness, schizophrenic reaction, seizures, somnolence, stroke (elderly), suicidal ideation, tardive dyskinesia, transient ischemic attack (elderly), tremor
CV: Arrhythmias, bradycardia, cardiopulmonary arrest, chest pain, circulatory collapse, deep vein thrombosis, elevated serum CK levels, heart failure, hypertension, MI, orthostatic hypotension, peripheral edema, prolonged QT interval, tachycardia
EENT: Blurred vision, conjunctivitis, dry mouth, hepatitis, increased salivation, laryngospasm, nasopharyngitis, oropharyngeal spasm, pharyngitis, rhinitis, sinusitis
ENDO: Hyperglycemia
GI: Abdominal discomfort, constipation, decreased appetite, diarrhea, difficulty swalaripiprazole 100 lowing, GI bleeding, indigestion, jaundice, nausea, vomiting
GU: Renal failure, urinary incontinence
HEME: Agranulocytosis, anemia, leukopenia, neutropenia, thrombocytopenia
MS: Arthralgia, elevated blood CK level, muscle spasms, muscleskeletal pain, myalgia, neck and limb rigidity, rhabdomyolysis
RESP: Apnea, aspiration, asthma, cough, dyspnea, pneumonia, pulmonary edema or embolism, respiratory failure
SKIN: Diaphoresis, dry skin, ecchymosis, pruritus, rash, ulceration, urticaria
Other: Anaphylaxis, angioedema, dehydration, flulike symptoms, heat stroke, weight gain

Cautions

Aripiprazole shouldn’t be used to treat dementia-related psychosis in the elderly because of an increased risk of death.

Use cautiously in patients with CV disease, cerebrovascular disease, or conditions that would predispose them to hypotension. Also use cautiously in those with a history of seizures or with conditions that lower the seizure threshold, such as Alzheimer’s disease.

Also use cautiously in elderly patients because of increased risk of serious adverse cerebrovascular effects, such as stroke and transient ischemic attack.

Oral solution may be given on a milligram-per-milligram basis in place of tablets up to 25 mg. For example, if patient needs 30 mg of tablet and is switched to oral solution, expect to give 25 mg of solution.

Inject parenteral form slowly, deep into the muscle, and never I.V. or subcutaneously.

Monitor patient for difficulty swallowing or excessive somnolence, which could predispose to accidental injury or aspiration.
WARNING Aripiprazole rarely may cause neuroleptic malignant syndrome, tardive dyskinesia, and seizures. Monitor patient closely throughout therapy, and take safety precautions as needed.

Monitor patient’s blood glucose level routinely; risk of hyperglycemia may increase.

Watch patients closely (especially children, adolescents, and young adults) for suicidal tendencies, particularly when therapy starts and dosage changes, because depression may worsen temporarily during these times.

Monitor patient’s CBC, as ordered, because serious adverse hematologic reactions may occur, such as agranulocytosis, leukopenia, and neutropenia. Assess more often during first few months of therapy if patient has a history of drug-induced leukopenia or neutropenia or a significantly low WBC count. If abnormalities occur during therapy, watch for fever or other signs of infection, notify prescriber and, if severre, expect drug to be stopped.

PATIENT SAFTY

Instruct patient prescribed orally disintegrating tablets to open the blister pack only when ready to take the tablet. Tell him to peel back the foil and not to push tablet through the foil because doing so could damage the tablet. Tell him to place the tablet on his tongue without breaking it and let it dissolve. If needed, he may take a drink.

Advise patient to get up slowly from a lying or sitting position during aripiprazole therapy to minimize orthostatic hypotension.

Urge patient to avoid alcohol during aripiprazole therapy.

Instruct patient to avoid hazardous activities until drug’s effects are known.

Urge patient to avoid activities that raise body temperature suddenly, such as strenuous exercise and exposure to extreme heat, and to compensate for situations that cause dehydration, such as vomiting or diarrhea.

Instruct patient to inform all prescribers of any he’s taking, including OTC , because of risk of interactions.

Advise female patient of childbearing age to notify prescriber if she intends to become or suspects that she is pregnant during therapy.

Instruct diabetic patient taking the oral solution to monitor blood glucose levels closely because each milliliter of solution contains 400 mg of sucrose and 200 mg of fructose.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes and particularly if patient is a child, teenager, or young adult.

Category

Chemical class: Diphenylmethyl sulfinylacetamide
Therapeutic class: CNS stimulant

Pregnancy category: C

Indications

To treat narcolepsy or as adjunct to standard therapy for excessive daytime sleepiness in obstructive sleep apnea/ hypopnea syndrome
Adults. 150 or 250 mg once daily in the morning. To improve daytime wakefulness in patients with excessive sleepiness from circadian rhythm disruption (shift-work sleep disorder)
Adults.150 mg once daily about 1 hr before start of work shift.
DOSAGE ADJUSTMENT Decreased dosage recommended for patients who are elderly, have severe hepatic impairment, or take steroidal contraceptives. Route Onset Peak Duration P.O. Unknown 2 hr Unknown (fasting) 4–6 hr (with food)

Mechanism of Action

May produce CNS-stimulant effects by binding to dopamine transporter in the brain and inhibiting dopamine reuptake in limbic regions. These actions increase alertness and reduce drowsiness and fatigue.

Contraindications

Hypersensitivity to armodafinil, modafinil, or their components

Interactions

amitriptyline, citalopram, clomipramine, diazepam, imipramine, propranolol, tolbutamide, topiramate: Possibly prolonged elimination time and increased blood levels of these barbiturates (such as phenobarbital, primidone), dexamethasone, rifabutin,
rifampin: Possibly decreased blood level and effectiveness of armodafinil carbamazepine: Possibly decreased armodafinil effectiveness and decreased blood carbamazepine level cimetidine, clarithromycin, erythromycin, fluconazole, fluoxetine, fluvoxamine, itraconazole, ketoconazole, nefazodone, sertraline: Possibly inhibited metabolism, decreased clearance, and increased blood level of armodafinil clozapine: Possibly increased levels of clozapine caused by decreased secondary hepatic metabolism contraceptive-containing implants or devices: Possibly contraceptive failure cyclosporine: Possibly decreased blood cyclosporine level and increased risk of organ transplant rejection dextroamphetamine,
methylphenidate: Possibly 1-hr delay in armodafinil absorption when these are given together fosphenytoin, mephenytoin,
phenytoin: Possibly decreased effectiveness of armodafinil, increased blood phenytoin level, and increased risk of phenytoin toxicity midazolam, triazolam: Possibly decreased effectiveness of triazolam or midazolam oral contraceptives: Possibly decreased effectiveness of oral contraceptive
theophylline: Possibly decreased blood level and effectiveness of theophylline
warfarin: Possibly decreased warfarin metabolism and increased risk of bleeding
alcohol use: Possibly adverse CNS effects all : 2to 4-hr delay for armodafinil to reach peak levels and possibly delayed onset of action caffeine: Increased CNS stimulation grapefruit juice: Possibly decreased armodafinil metabolism

Side Efect

CNS: Agitation, anxiety, attention disturbance, depression, dizziness, fatigue, fever, headache (including migraine), insomnia, nervousness, paresthesia, suicidal ideation, thirst, tremor
CV: Increased heart rate, palpitations
EENT: Dry mouth
GI: Abdominal pain (upper), anorexia, conarmodafinil 102 stipation, decreased appetite, diarrhea, dyspepsia, loose stools, nausea, vomiting
GU: Polyuria
RESP: Dyspnea
SKIN: Contact dermatitis, hyperhydrosis, rash
Other: Angioedema, flulike illness

Cautions

Armodafinil shouldn’t be given to patients with mitral valve prolapse syndrome or a history of left ventricular hypertrophy because drug may cause ischemic changes.
WARNING If patient has a history of alcoholism, stimulant abuse, or other substance abuse, ensure compliance with armodafinil therapy. Watch for signs of misuse or abuse, including frequent prescription refill requests, increased frequency of dosing, and drug-seeking behavior. Also watch for evidence of excessive armodafinil use, including agitation, anxiety, diarrhea, nausea, nervousness, palpitations, sleep disturbances, and tremor.

Be aware that armodafinil, like other CNS stimulants, may alter mood, perception, thinking, judgment, feelings, and motor skills and may produce signs that patient needs sleep.

If giving drug to patient with a history of psychosis, emotional instability, or psychological illness with psychotic features, be prepared for baseline behavioral assessment or frequent clinical observation.

PATIENT SAFTY

Inform patient that armodafinil can help, but not cure, narcolepsy and that drug’s full effects may not be seen right away.

Advise patient to avoid taking armodafinil within 2 hours of eating because food may delay time to peak drug effect and onset of action. If patient drinks grapefruit juice, encourage him to drink a consistent amount daily.

Inform patient that drug can affect his concentration and ability to function and can hide signs of fatigue. Urge him not to drive or perform activities that require mental alertness until drug’s full CNS effects are known.

Because alcohol may decrease alertness, advise patient to avoid it with armodafinil.

Encourage a regular sleeping pattern.

Caution patient to avoid excessive intake of , beverages, and OTC that contain caffeine because caffeine may lead to increased CNS stimulation.

Inform woman that armodafinil can decrease effectiveness of certain contraceptives, including birth control pills and implantable hormonal contraceptives. If she uses such contraceptives, urge her to use an alternate birth control method during armodafinil therapy and for up to 1 month after it stops.

Advise patient to keep follow-up appointments with prescriber so that her progress can be monitored.

Category

Chemical: Dibenzo-oxepino pyrrole Therapeutic: Second-generation antipsychotic, atypical antipsychotic

Pregnancy category: C

Indications

To treat schizophrenia SUBLINGUAL
Adults. 5 mg twice daily. To treat manic or mixed episodes associated with bipolar I disorder SUBLINGUAL
Adults. 10 mg twice daily.
DOSAGE ADJUSTMENT Dosage may be decreased to 5 mg twice daily if adverse reactions occur. Route Onset Peak Duration P.O. Unknown 30–90 min Unknown

Mechanism of Action

May produce antipsychotic effects through antagonist actions at dopamine receptors, especially D2, and serotonin receptors, especially 5-HT2A.

Contraindications

Hypersensitivity to asenapine or its components

Interactions

antihypertensives,
CNS depressants: Possibly enhanced effects class I A and III antiarrhythmics, gatifloxacin, moxifloxacin, other antipsychotic : Increased risk of prolonged QT interval paroxetine: Possibly increased paroxetine effect
alcohol use: Possibly enhanced effect

Side Efect

CNS: Akathisia, anxiety, depression, dizziness, dystonia, dyskinesia, extrapyramidal symptoms, fatigue, gait disturbance, hyperkinesias, insomnia, irritability, masked facies, parkinsonism, seizures, somnolence, syncope, tardive dyskinesia, torticollis, tremor
CV: Hypertension, orthostatic hypotension, prolonged QT interval
EENT: Blepharospasm, dry mouth, oral hypoesthesia, salivary hypersecretion, toothache
ENDO: Hyperglycemia, hyperprolactinemia
GI: Constipation, dyspepsia, increased appetite, stomach discomfort, vomiting
HEME: Anemia, leukopenia, neutropenia, thrombocytopenia
MS: Arthralgia, extremity pain, muscle rigidity
Other: Hyponatremia, weight gain

Cautions

Asenapine should be avoided in patients with a history of cardiac arrhythmias; conditions that might prolong the QT interval, such as bradycardia, hypokalemia, or hypomagnesemia; or congenital QT-interval prolongation because of increased risk of torsades de pointes or sudden death.

Asenapine shouldn’t be used for dementia-related psychosis in elderly patients because of an increased risk of death.

Use cautiously in patients with mild to moderate hepatic impairment. Asenapine isn’t recommended in patients with severe hepatic impairment (Child-Pugh Class C).

Use cautiously in patients with a history of seizures or who have conditions that may lower the seizure threshold, such as Alzheimer’s dementia, because drug increases risk of seizures in these patients.

Monitor patients with diabetes mellitus for increased blood glucose levels.
WARNING Asenapine rarely may cause neuroleptic malignant syndrome or tardive dyskinesia. Monitor patient closely throughout therapy, and take safety precautions as needed. Expect to stop drug if any of these adverse effects occur.

Monitor patient’s CBC regularly, as ordered. Notify prescriber of any change because drug may need to be stopped.

Monitor patient for trouble swallowing or excessive somnolence, which could predispose him to injury or aspiration.

PATIENT SAFTY

Tell patient to remove tablet from package only when ready to take it and to use dry hands. Tell him to firmly press and hold thumb button, and then pull out tablet pack from case. Then, he should peel back the colored tab, being careful not to push tablet through the tab because doing so could damage tablet. Instruct patient to place tablet under his tongue and let it dissolve completely. Tell him to then slide tablet pack back into case until it clicks.

Caution patient not to crush, chew or swallow tablets.

Advise him not to eat or drink for at least 10 minutes after taking asenapine.

Urge patient to avoid alcohol while taking asenapine.

Instruct diabetic patient taking asenapine to monitor blood glucose levels closely because hyperglycemia may occur.

Advise patient to get up slowly from lying or sitting position during asenapine therapy to minimize orthostatic hypotension.

Caution patient to avoid hazardous activities until drug’s effects are known.

Urge patient to avoid activities that raise body temperature suddenly, such as strenuous exercise and exposure to extreme heat, and to compensate for situations that cause dehydration, such as vomiting or diarrhea.

Category

Chemical class: Salicylate
Therapeutic class: Anti-inflammatory, antiplatelet, antipyretic, nonopioid analgesic

Pregnancy category: D

Indications

To relieve mild pain or fever CHEWABLE , CHEWING GUM, CONTROLLEDRELEASE , ENTERIC-COATED , SOLUTION,,TIMED-RELEASE , SUPPOSITORIES Adults and adolescents. 325 to 650 mg every 4 hr, p.r.n., or 500 mg every 3 hr, p.r.n., or 1,000 mg every 6 hr, p.r.n. Children ages 2 to 14. 10 to 15 mg/kg/dose every 4 hr, p.r.n., up to 80 mg/kg daily. To relieve mild to moderate pain from inflammation, as in rheumatoid arthritis and osteoarthritis CHEWABLE ,CHEWING GUM,CONTROLLEDRELEASE ,ENTERIC-COATED , SOLUTION,,TIMED-RELEASE , SUPPOSITORIES Adults and adolescents. 3.2 to 6 g daily in divided doses. Maximum: 6 g daily. Children.10 to 15 mg/kg daily, up to 80 mg/ kg daily, in divided doses every 4 to 6 hr. To treat juvenile rheumatoid arthritis CHEWABLE , CHEWING GUM, CONTROLLEDRELEASE , ENTERIC-COATED , SOLUTION,,TIMED-RELEASE , SUPPOSITORIES Children.60 to 110 mg/kg daily in divided doses every 6 to 8 hr. To treat acute rheumatic fever CHEWABLE ,CHEWING GUM,CONTROLLEDRELEASE ,ENTERIC-COATED , SOLUTION,,TIMED-RELEASE , SUPPOSITORIES Adults and adolescents.5 to 8 g daily in divided doses. Children.Initial: 100 mg/kg daily in divided doses for first 2 wk. Maintenance: 75 mg/ kg/day in divided doses for next 4 to 6 wk. To reduce the risk of recurrent transient ischemic attacks or stroke in men CHEWABLE ,CHEWING GUM,CONTROLLEDRELEASE ,ENTERIC-COATED , SOLUTION,,TIMED-RELEASE , SUPPOSITORIES
Adults.650 mg b.i.d. or 325 mg q.i.d. To reduce the severity of or prevent acute MI CHEWABLE ,CHEWING GUM,CONTROLLEDRELEASE ,ENTERIC-COATED , SOLUTION,,TIMED-RELEASE , SUPPOSITORIES
Adults. Initial: 160 to 162.5 mg (half of a 325-mg tablet or two 80or 81-mg tablets) as soon as MI is suspected. Maintenance: 160 to 162.5 mg daily for 30 days. To reduce risk of MI in patients with previous MI or unstable angina CHEWABLE ,CHEWING GUM,CONTROLLEDRELEASE ,ENTERIC-COATED , SOLUTION,,TIMED-RELEASE , SUPPOSITORIES
Adults. 325 mg daily. Route Onset Peak Duration P.O. Rapid Unknown 1–4 hr (chewable tablets) P.O. 5–30 1–4 hr 4–6 hr (controlled-min release) P.O. 5–30 Unknown 1–4 hr (entericmin coated) P.O. 5–30 15–40 1–4 hr (solution) min min P.O. 15–30 1–2 hr 4 –6 hr (tablets) min P.O. 5–30 1–4 hr 4–6 hr (timedmin release) P.R. Unknown Unknown 4–6 hr

Mechanism of Action

Blocks the activity of cyclooxygenase, the enzyme needed for prostaglandin synthesis. Prostaglandins, important mediators in the inflammatory response, cause local vasodilation with swelling and pain. With blocking of cyclooxygenase and inhibition of prostaglandins, inflammatory symptoms subside. Pain is also relieved because prostaglandins play a role in pain transmission from the periphery to the spinal cord. Aspirin inhibits platelet aggregation by interfering with production of thromboxane A2, a substance that stimulates platelet aggregation. Aspirin acts on the heatregulating center in the hypothalamus and causes peripheral vasodilation, diaphoresis, and heat loss.

Contraindications

Allergy to tartrazine dye, asthma, bleeding problems (such as hemophilia), hypersensitivity to aspirin or its components, peptic ulcer disease

Interactions

ACE inhibitors: Decreased antihypertensive effect activated charcoal: Decreased aspirin absorption antacids, urine alkalinizers: Decreased aspirin effectiveness anticoagulants: Increased risk of bleeding; prolonged bleeding time carbonic anhydrase inhibitors: Salicylism corticosteroids: Increased excretion and decreased blood level of aspirin heparin: Increased risk of bleeding ibuprofen: Possibly reduced cardioprotective and stroke preventive effects of aspirin methotrexate: Increased blood level and decreased excretion of methotrexate, causing toxicity nizatidine: Increased blood aspirin level
NSAIDs: Possibly decreased blood NSAID level and increased risk of adverse GI effects sulfonylureas: Possibly enhanced effect of sulfonylureas with large doses of aspirin urine acidifiers (such as ammonium chloride, ascorbic acid): Decreased aspirin excretion vancomycin: Increased risk of ototoxicity
alcohol use: Increased risk of ulcers

Side Efect

CNS: Confusion, CNS depression
EENT: Hearing loss, tinnitus
GI: Diarrhea, GI bleeding, heartburn, hepatotoxicity, nausea, stomach pain, vomiting
HEME: Decreased blood iron level, leukopenia, prolonged bleeding time, shortened life span of RBCs, thrombocytopenia
SKIN: Ecchymosis, rash, urticaria
Other: Angioedema, Reye’s syndrome, salicylism (dizziness, tinnitus, difficulty hearing, vomiting, diarrhea, confusion, CNS depression, diaphoresis, headache, hyperventilation, and lassitude) with regular use of large doses

Cautions

Don’t crush timed-release or controlledrelease aspirin tablets unless directed.

Ask about tinnitus. This reaction usually occurs when blood aspirin level reaches or exceeds maximum for therapeutic effect.

PATIENT SAFTY

WARNING Advise parents not to give aspirin to a child or adolescent with chickenpox or flu symptoms because of risk of Reye’s syndrome (rare life-threatening reaction characterized by vomiting, lethargy, belligerence, delirium, and coma). Tell them to consult prescriber for alternative .

Advise adult patient taking low-dose aspirin not to also take ibuprofen because it may reduce the cardioprotective and stroke preventive effects of aspirin.

Instruct patient to take aspirin with food or after meals because it may cause GI upset if taken on an empty stomach.

Advise patient with tartrazine allergy not to take aspirin.

Tell patient to consult prescriber before taking aspirin with any prescription drug for blood disorder, diabetes, gout, or arthritis.

Tell patient not to use aspirin if it has a strong vinegar-like odor.

Category

Chemical class: Beta-adrenergic blocker (beta1and at high doses beta2)
Therapeutic class: Antianginal, antihypertensive

Pregnancy category: D

Indications

To treat angina pectoris and control hypertension
Adults.50 mg daily increased, p.r.n., after 1 to 2 wk to 100 mg daily. To treat acute MI atenolol 106 ,
IV:
Adults. Initial: 5 mg I.V. over 5 min followed by 5 mg I.V. 10 min later. After another 10 min, 50 mg given and followed by another 50 mg in 12 hr. Maintenance: 50 mg P.O. b.i.d. or 100 mg P.O. daily for 6 to 9 days or until discharged from hospital.
DOSAGE ADJUSTMENT Dosage reduced to 50 mg daily P.O. for renally impaired patients and for elderly, renally impaired patients with creatinine clearance of 15 to 35 ml/min/1.73 m2. Dosage reduced to 25 mg daily P.O. for renally impaired patients and for elderly, renally impaired patients with creatinine clearance less than 15 ml/min/1.73 m2. Route Onset Peak Duration P.O. 1 hr 2–4 hr 24 hr I.V. Immediate 5 min 12 hr

Mechanism of Action

Inhibits stimulation of beta1-receptor sites, located mainly in the heart, decreasing cardiac excitability, cardiac output, and myocardial oxygen demand. Atenolol also acts to decrease release of renin from the kidneys, aiding in reducing blood pressure. At high doses, it inhibits stimulation of beta2 receptors in the lungs, which may cause bronchoconstriction.

Contraindications

Cardiogenic shock, heart block greater than first degree, hypersensitivity to beta blockers, overt heart failure, sinus bradycardia

Interactions

amiodarone: Additive atenolol effects calcium channel blockers, such as verapamil and diltiazem: Possibly symptomatic bradycardia and conduction abnormalities catecholamine-depleting , such as reserpine: Additive antihypertensive effect
clonidine: Rebound hypertension disopyramide: Increased risk of severe bradycardia, asystole, and heart failure

Side Efect

CNS: Depression, disorientation, dizziness, drowsiness, emotional lability, fatigue, fever, lethargy, light-headedness, short-term memory loss, vertigo
CV: Arrhythmias, including bradycardia and heart block; cardiogenic shock; cold arms and legs; heart failure; mesenteric artery thrombosis; mitral insufficiency; myocardial reinfarction; orthostatic hypotension; Raynaud’s phenomenon
EENT: Dry eyes, laryngospasm, pharyngitis
GI: Diarrhea, ischemic colitis, nausea
GU: Renal failure
HEME: Agranulocytosis
MS: Leg pain
RESP: Bronchospasm, dyspnea, pulmonary emboli, respiratory distress, wheezing
SKIN: Erythematous rash
Other: Allergic reaction

Cautions

Use atenolol cautiously in patients with heart failure controlled by digitalis glycosides or diuretics, patients with conduction abnormalities or left ventricular dysfunction who take verapamil or diltiazem, patients with arterial circulatory disorders, and patients with impaired renal function.

Use atenolol cautiously in diabetic patients because it may mask tachycardia caused by hypoglycemia. Unlike other beta-adrenergic blockers, it doesn’t mask other signs of hypoglycemia, cause hypoglycemia, or delay the return of blood glucose to a normal level.

At first sign of heart failure, expect patient to receive a digitalis glycoside, a diuretic, or both and to be monitored closely. If failure continues, expect to stop atenolol.

Closely monitor patient with hyperthyroidism because atenolol may mask some signs of thyrotoxicosis. Abrupt withdrawal of atenolol may precipitate thyrotoxicosis.

If patient also receives clonidine, expect to stop atenolol several days before gradually withdrawing clonidine. Then expect to restart atenolol therapy several days after clonidine has been discontinued.

During I.V. atenolol therapy, monitor vital signs and cardiac rhythm closely.

Discard parenteral mixture with atenolol if it isn’t used within 48 hours.

Stop atenolol and notify prescriber if patient develops bradycardia, hypotension, or other serious adverse reaction.

PATIENT SAFTY

Instruct patient not to stop taking atenolol abruptly. Otherwise, angina may worsen, and an MI or arrhythmia may occur.

While patient is being weaned from atenolol, tell him to perform minimal physical activity to prevent chest pain.

Instruct patient to take a missed dose as soon as possible. However, if it’s within 8 hours of the next scheduled dose, tell him to skip the missed dose and return to his regular schedule.

Explain that atenolol may alter serum glucose level and mask hypoglycemia.

Inform the patient that he may experience fatigue and reduced tolerance to exercise and that he should notify his prescriber if this interferes with his normal lifestyle.

Category

Chemical class: Selective norepinephrine reuptake inhibitor
Therapeutic class: Anti–ADHD agent

Pregnancy category: C

Indications

To treat attention deficit hyperactivity disorder (ADHD) Adults and children weighing 70 kg (154 lb) or less. Initial: 0.5 mg/kg daily, increased after at least 3 days to 1.2 mg/kg daily given either as a single dose in the morning or in evenly divided doses morning and late afternoon or early evening, as needed. Maximum: 1.4 mg/kg or 100 mg daily, whichever is less. Adults and children weighing more than 70 kg.Initial: 40 mg daily, increased after at least 3 days to 80 mg daily given either as a single dose in the morning or in evenly divided doses morning and late afternoon or early evening. After 2 to 4 additional wk, dosage may be increased to 100 mg daily if optimal response hasn’t been achieved. Maximum: 100 mg daily.
DOSAGE ADJUSTMENT For patients with moderate (Child-Pugh Class B) hepatic impairment, dosage reduced by 50%. For patients with severe (Child-Pugh Class C) hepatic impairment, dosage reduced by 75%. For patients weighing 70 kg or less and taking strong CYP2D6 inhibitors, such as paroxetine, fluoxetine, or quinidine, initial dosage of 0.5 mg/kg daily should be increased to 1.2 mg/kg daily only if symptoms fail to improve after 4 wk. For patients weighing more than 70 kg and taking strong CYP2D6 inhibitors, initial dosage of 40 mg daily should be increased to 80 mg daily only if symptoms fail to improve after 4 wk.

Mechanism of Action

Selectively inhibits presynaptic norepinephrine transport in the nervous system to increase attention span and produce a calming effect.

Contraindications

Angle-closure glaucoma, hypersensitivity to atomoxetine or its components, use within 14 days of MAO inhibitor therapy

Interactions

albuterol and other beta2agonists: May potentiate action of albuterol and other beta2agonists on cardiovascular system CYP2D6 inhibitors (such as fluoxetine, paroxetine, and quinidine): Increased blood atomoxetine level
MAO inhibitors: Possibly induced hypertensive crisis pressor agents: Possibly altered blood pressure

Side Efect

CNS: Aggressiveness, anxiety, chills, crying, depression, dizziness, early morning awakening, fatigue, headache, hostility, insomnia, irritability, lethargy, mood changes, paresthesia, peripheral coldness, pyrexia, rigors, sedation, seizures, sleep disturbance, somnolence, stroke, suicidal ideation (children and adolescents), syncope, tremor, unusual dreams
CV: Chest pain, hypertension, orthostatic hypotension, MI, palpitations, QT-interval prolongation, Raynaud’s phenomenon, tachycardia
EENT: Conjunctivitis, dry mouth, ear infection, mydriasis, nasal congestion, nasopharyngitis, pharyngitis, rhinorrhea, sinus congestion
ENDO: Hot flashes
GI: Abdominal pain (upper), anorexia, constipation, diarrhea, elevated liver function atomoxetine hydrochloride 108 test results, flatulence, gastroenteritis (viral), indigestion, nausea, severe hepatic dysfunction, vomiting
GU: Decreased libido, dysmenorrhea, dysuria, ejaculation disorders, erectile dysfunction, impotence, male pelvic pain, menstrual irregularities, orgasm abnormality, priapism, prostatitis, urinary hesitancy, urine retention
MS: Arthralgia, back pain, myalgia
RESP: Cough, upper respiratory tract infection
SKIN: Dermatitis, diaphoresis, pruritus, rash, urticaria
Other: Angioedema, influenza, weight loss

Cautions

Use atomoxetine cautiously in patients with cerebrovascular or CV disease (especially hypertension or tachycardia) because drug may increase blood pressure and heart rate. Also use cautiously in those prone to orthostatic hypotension and those with serious structural cardiac abnormlities, cardiomyopathy, serious heart rhythm abnormalities, or other serious cardiac problems because drug may increase risk of sudden death from these conditions.
WARNING Monitor children and adolescents closely for evidence of suicidal thinking and behavior as well as for psychotic or manic symptoms such as hallucinations, delusional thinking, or mania because atomoxetine increases the risk of suicidal ideation and the onset of psychotic or manic symptoms in these age-groups.

Obtain baseline blood pressure and heart rate before starting therapy. Monitor patient’s vital signs after dosage increases and periodically during therapy.

Monitor patient closely for allergic reactions. If these occur, notify prescriber.

Monitor child’s or adolescent’s growth and weight. Expect to interrupt therapy, as prescribed, if patient isn’t growing or gaining weight appropriately.

Monitor patient’s liver function studies, as ordered. Notify prescriber immediately if enzyme levels are elevated or patient has evidence of hepatic dysfunction (jaundice, dark urine, pruritus, right-upper-quadrant tenderness, or unexplained flulike symptoms). Expect to stop drug permanently.

PATIENT SAFTY

Caution patient not to open capsules. If a capsule opens, urge patient to promptly wash his hands and any surface drug touches. If drug gets in his eyes, tell him to flush immediately with water and seek medical care.

Instruct patient or parent to immediately report to prescriber any

Side Efect

to atomoxetine therapy, such as facial swelling, itching, or rash.
WARNING Urge parents to watch their child or adolescent closely for evidence of abnormal thinking or behavior or increased aggression or hostility. Stress need to notify prescriber about unusual changes.

Urge patient to tell prescriber immediately about yellowing of his skin or eyes, itchiness, right upper abdominal pain, dark urine, or flulike symptoms. Also tell patient to notify prescriber immediately if he experiences exertional chest pain, unexplained syncope, or other symptoms suggestive of heart disease.

Caution patient to assume sitting or standing position slowly because of drug’s potential effect on blood pressure.

Urge male patient to seek immediate medical attention for a penile erection that becomes prolonged or painful.

Advise patient to report urinary hesitancy or urine retention to prescriber.

Remind patient of the importance of alerting all prescribers to any OTC , dietary supplements, or herbal remedies he’s taking.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Reassure patient or parent that drug doesn’t cause physical or psychological dependence.

Instruct patient or parent to monitor weight during therapy.

Category

Chemical class: Synthetically derived fermentation product
Therapeutic class: Antihyperlipidemic, HMG-CoA reductase inhibitor

Pregnancy category: X

Indications

To control lipid levels as adjunct to diet in primary (heterozygous familial and nonfamilial) hypercholesterolemia and mixed dyslipidemia
Adults.Initial: 10 or 20 mg once daily; then increased according to lipid level. Maintenance: 10 to 80 mg once daily.
DOSAGE ADJUSTMENT Initial dose may be increased to 40 mg once daily for patients who need cholesterol level reduced more than 45%. To control lipid levels in homozygous familial hypercholesterolemia
Adults.10 to 80 mg daily. To control lipid levels in pediatric heterozygous familial hypercholesterolemia Adolescents and children ages 10 to 17. Initial: 10 mg daily, adjusted at intervals of 4 wk or more, as needed. Maximum: 20 mg daily. To reduce debilitating cardiovascular events such as stroke and MI in patients with multiple risk factors but without known coronary artery disease
Adults. 10 mg once daily.

Mechanism of Action

Reduces plasma cholesterol and lipoprotein levels by inhibiting HMG-CoA reductase and cholesterol synthesis in the liver and by increasing the number of LDL receptors on liver cells to enhance LDL uptake and breakdown.

Contraindications

Active hepatic disease, hypersensitivity to atorvastatin or its components, unexplained persistent rise in serum transaminase level

Interactions

amlodipine, cimetidine, clarithromycin, diltiazem, erythromycin, itraconazole, ritonavir with saquinavir: Increased atorvastatin level antacid, colestipol, efavirenz,
rifampin: Possibly decreased blood atorvastatin level azole antifungals, clarithromycin, cyclosporine, erythromycin, fibric acid derivatives, lopinavir with ritonavir, niacin (at dosage used for lipid modification), nicotinic acid, ritonavir with saquinavir: Increased risk of severe myopathy or rhabdomyolysis cyclosporine: Increased atorvastatin bioavailability and risk of

Side Efect

digoxin: Possibly increased blood digoxin level, causing toxicity oral contraceptives (such as ethinyl estradiol and norethindrone): Increased hormone level grapefruit juice (more than 1.2 L daily): Increased blood atorvastatin level

Side Efect

CNS: Abnormal dreams, amnesia, asthenia, emotional lability, facial paralysis, fever, headache, hyperkinesia, lack of coordination, malaise, paresthesia, peripheral neuropathy, somnolence, syncope, weakness
CV: Arrhythmias, elevated serum CK level, orthostatic hypotension, palpitations, phlebitis, vasodilation
EENT: Amblyopia, altered refraction, dry eyes, dry mouth, epistaxis, eye hemorrhage, gingival hemorrhage, glaucoma, glossitis, hearing loss, lip swelling, loss of taste, pharyngitis, sinusitis, stomatitis, taste perversion, tinnitus
ENDO: Hyperglycemia or hypoglycemia
GI: Abdominal or biliary pain, anorexia, colitis, constipation, diarrhea, duodenal or stomach ulcers, dysphagia, eructation, esophagitis, flatulence, gastroenteritis, hepatic failure, hepatitis, increased appetite, indigestion, melena, pancreatitis, rectal hemorrhage, tenesmus, vomiting
GU: Abnormal ejaculation; cystitis; decreased libido; dysuria; epididymitis; hematuria; impotence; nephritis; nocturia; renal calculi; urinary frequency, incontinence, or urgency; urine retention; vaginal hemorrhage
HEME: Anemia, thrombocytopenia
MS: Arthralgia, back pain, bursitis, gout, leg cramps, myalgia, myasthenia gravis, myositis, neck rigidity, tendon contracture, tenosynovitis, torticollis
RESP: Dyspnea, pneumonia
SKIN: Acne, alopecia, contact dermatitis, diaphoresis, dry skin, ecchymosis, eczema, jaundice, petechiae, photosensitivity, pruritus, rash, seborrhea, ulceration, urticaria atorvastatin calcium 110
Other: Allergic reaction, facial or generalized edema, flulike symptoms, infection, lymphadenopathy, weight gain

Cautions

Atorvastatin is used in patients with homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering treatments or alone only if other treatments aren’t available.

Atorvastatin may be used with colestipol or cholestyramine for additive antihyperlipidemic effects.

Expect atorvastatin to be used in patients without obvious coronary artery disease (CAD) but with multiple risk factors (such as age 55 or over, smoker, history of hypertension or low HDL level, or family history of early CAD). Drug is used to reduce risk of MI, angina, and adverse effects of revascularization procedures.

Also expect drug to be used in patients with type 2 diabetes who have no obvious CAD but multiple risk factors, such as retinopathy, albuminuria, smoking, or hypertension. Drug is used in these patients to reduce risk of MI and stroke.

Expect liver function tests to be performed before atorvastatin therapy starts, after 6 and 12 weeks, with each dosage increase, and every 6 months thereafter.

Expect to measure lipid levels 2 to 4 weeks after therapy starts, to adjust dosage as directed, and to repeat periodically until lipid levels are within desired range.

PATIENT SAFTY

Stress that atorvastatin is an adjunct to— not a substitute for—low-cholesterol diet.

Tell patient to take drug at the same time each day to maintain its effects.

Instruct patient to take a missed dose as soon as possible. If it’s almost time for his next dose, he should skip the missed dose. Tell him not to double the dose.

Instruct patient to consult prescriber before taking OTC niacin because of increased risk of rhabdomyolysis.

Advise patient to notify prescriber immediately if he develops unexplained muscle pain, tenderness, or weakness, especially if accompanied by fatigue or fever.

Be aware that atorvastatin is expensive. Reinforce the benefits of therapy, and urge patient to comply if possible.

Category

Chemical class: Hydroxy-1,4-naphthoquinone
Therapeutic class: Antiprotozoal

Pregnancy category: C

Indications

To prevent Pneumocystis jiroveci (formerly carinii) pneumonia in patients who can’t tolerate co-trimoxazole SUSPENSION, Adults and adolescents.750 mg (5 ml) b.i.d. with meals for 21 days. To treat mild to moderate P. jiroveci pneumonia in patients who can’t tolerate co-trimoxazole SUSPENSION, Adults and adolescents.750 mg (5 ml) b.i.d. with meals for 21 days. Maximum: 1,500 mg/day.

Mechanism of Action

May destroy P. jiroveci organisms by inhibiting the enzymes needed to synthesize nucleic acid and adenosine triphosphate.

Contraindications

Hypersensitivity to atovaquone or its components

Interactions

rifabutin,
rifampin: Possibly decreased blood atovaquone level

Side Efect

CNS: Fever, headache, insomnia
EENT: Rhinitis, throat tightness, vortex keratopathy
GI: Abdominal pain, diarrhea, elevated liver enzyne levels, hepatitis, hepatic failure, nausea, pancreatitis, vomiting
GU: Acute renal dysfunction
HEME: Anemia, thrombocytopenia
RESP: Bronchospasm, cough, dyspnea
SKIN: Desquamation, erythema multiforme, Stevens-Johnson syndrome, rash, urticaria
Other: Allergic reaction, angioedema, methemoglobinemia

Cautions

Use atovaquone cautiously in patient with severe hepatic impairment because, although rare, serious

Side Efect

affecting liver function may occur.

Monitor blood test results because atovaquone may decrease serum sodium and hemoglobin levels and neutrophil count and may increase AST, ALT, alkaline phosphatase, and serum amylase levels.

Crush atovaquone tablets, if needed.

Don’t use tablets and oral suspension interchangeably; they aren’t bioequivalent.

PATIENT SAFTY

Instruct patient to take atovaquone with meals for maximum effectiveness.

Instruct patient to take a missed dose as soon as possible. If it’s almost time for the next dose, tell him to skip the missed dose. Tell him not to double the next dose.

Tell patient to notify prescriber if his condition doesn’t improve in a few days or if he develops signs of an allergic reaction, such as fever or rash.

Category

Chemical class: Biquaternary ammonium ester
Therapeutic class: Skeletal muscle relaxant

Pregnancy category: C

Indications

To facilitate endotracheal intubation and induce skeletal muscle relaxation for surgery or mechanical ventilation as adjunct to anesthesia
IV: OR INJECTION Adults and children age 2 or over. Initial: 0.4 to 0.5 mg/kg by I.V. bolus for nearly complete neuromuscular blockade. Maintenance: 0.08 to 0.10 mg/kg 20 to 45 min after initial dose during prolonged surgery. Maintenance doses may be given every 15 to 25 min for patients under balanced anesthesia. For patients having extended surgical procedures, after an initial I.V. bolus, an infusion of 9 to 10 mcg/ kg/min may be needed to counteract the spontaneous return of neuromuscular function and thereafter 5 to 10 mcg/kg/min as a constant infusion. Children ages 1 month to 2 years having halothane anesthesia. Initial: 0.3 to 0.4 mg/ kg. Frequent maintenance doses may be needed. Route Onset Peak Duration I.V. 2–2.5 min 3–5 min 35–70 min

Mechanism of Action

Inhibits nerve impulse transmission by competing with acetylcholine for cholinergic receptors on motor end plate.

Incompatibilities

Don’t mix atracurium in same syringe or give it through same I.V. needle as an alkaline solution, such as a barbiturate injection. Don’t mix atracurium with lactated Ringer’s injection.

Contraindications

Hypersensitivity to atracurium, its components, or benzyl alcohol

Interactions

aminoglycosides, enflurane, furosemide, halothane, isoflurane, lithium, magnesium salts, polymyxin antibiotics, procainamide, quinidine, thiazide diuretics: Possibly enhanced or prolonged atracurium effects opioid analgesics: Possibly additive histamine release and increased risk and severity of bradycardia and hypotension

Side Efect

CNS: Seizures
CV: Bradycardia, hypertension, hypotension, tachycardia
MS: Inadequate or prolonged neuromuscular blockade
RESP: Apnea, bronchospasm, dyspnea, laryngospasm, wheezing
SKIN: Flushing, rash, urticaria
Other: Anaphylaxis, injection site reaction

Cautions

Use atracurium cautiously in patients with hypotension, and monitor blood pressure closely.

Watch closely for

Side Efect

, especially those related to histamine release. Atracurium is more likely than other neuromuscular blockers to cause skin flushing.

Anticipate using lower doses for patients with neuromuscular disease, severe elecatracurium besylate 112 trolyte disorders, or carcinomatosis because of risk of enhanced neuromuscular blockade and difficulties with reversal.

Keep atropine nearby to treat atracuriuminduced bradycardia.

For I.V. infusion, dilute atracurium with normal saline solution, D5W, or dextrose 5% in normal saline solution. To prepare a solution that yields 200 mcg/ml atracurium, add 2 ml atracurium to 98 ml diluent. To prepare a solution that yields 500 mcg/ ml, add 5 ml atracurium to 95 ml diluent.

Refrigerate solution or store at room temperature for up to 24 hours.

PATIENT SAFTY

Explain atracurium’s purpose and administration during anesthesia. Keep in mind that the patient can still hear.

Category

Chemical class: Belladonna alkaloid
Therapeutic class: Anticholinergic, antimuscarinic

Pregnancy category: C

Indications

To reduce respiratory tract secretions related to anesthesia (ATROPINE SULFATE)
Adults. 0.4 to 0.6 mg preoperatively. Children.0.01 mg/kg up to total of 0.4 mg preoperatively and repeated every 4 to 6 hr, p.r.n. I.V.,I.M., OR SUBCUTANEOUS INJECTION
Adults. 0.4 to 0.6 mg preoperatively. Children.0.01 mg/kg up to total of 0.4 mg preoperatively and repeated every 4 to 6 hr, p.r.n. To correct bradycardia
I.V.INJECTION(ATROPINE SULFATE)
Adults.0.4 to 1 mg. If no response to first dose, repeat once after 5 min. Children.0.01 to 0.02 mg/kg with a minimum dose of 0.1 mg and a maximum dose of 0.5 mg. If no response to first dose, repeat once after 5 min. To treat cholinesterase inhibitor (such as neostigmine, pilocarpine, and methacholine) toxicity
I.V.INJECTION(ATROPINE SULFATE)
Adults. 2 to 4 mg. Then 2 mg every 5 to 10 min until muscarinic signs (bradycardia, vasodilation, and pupil dilation) disappear or signs of atropine intoxication develop. I.V.OR
I.M.INJECTION(ATROPINE SULFATE) Children. 1 mg. Then 0.5 to 1 mg every 5 to 10 min until muscarinic signs disappear or signs of atropine intoxication develop. To treat mushroom (muscarine) toxicity I.V.OR
I.M.INJECTION(ATROPINE SULFATE)
Adults. 1 to 2 mg every hr until respiratory signs and symptoms subside. To treat pesticide (organophosphate) toxicity I.V. OR

IM

(ATROPINE SULFATE)
Adults. 1 to 2 mg, repeated in 20 to 30 min as soon as cyanosis has cleared. Then continued until definite improvement is maintained, possibly for 2 or more days. To treat known or suspected exposure to chemical nerve agent or insecticide

IM

(ATROPEN) Adults and children weighing over 41 kg (90 lb) with two or more mild symptoms. 2 mg. If severe symptoms develop after injection, two or more 2-mg injections given in rapid succession 10 min after initial injection. Adults and children weighing over 41 kg who are unconscious or have other severe symptoms.2 mg given immediately 3 times in rapid succession. Children weighing 18 to 41 kg (40 to 90 lb) with two or more mild symptoms. 1 mg. If severe symptoms develop after injection, two more 1-mg injections given in rapid succession 10 min after initial injection. Children weighing 18 to 41 kg who are unconscious or exhibit any other severe symptoms.1 mg given immediately 3 times in rapid succession. Children weighing 7 to 18 kg (15 to 40 lb) with two or more mild symptoms.0.5 mg. If severe symptoms develop after injection, two more 0.5-mg injections given in rapid succession 10 min after initial injection. Children weighing 7 to 18 kg who are unconscious or exhibit any other severe symptoms. 0.5 mg given immediately 3 times in rapid succession.

Mechanism of Action

Inhibits acetylcholine’s muscarinic action at the neuroeffector junctions of smooth muscles, cardiac muscles, exocrine glands, SA and AV nodes, and the urinary bladder. In small doses, atropine inhibits salivary and bronchial secretions and diaphoresis. In moderate doses, it increases impulse conduction through the AV node and increases heart rate. In large doses, it decreases GI and urinary tract motility and gastric acid secretion.

Contraindications

Angle-closure glaucoma, asthma, GI obstructive disease (achalasia, pyloric obstruction, pyloroduodenal stenosis), hepatic disease, hypersensitivity to atropine or its components, ileus, intestinal atony, myasthenia gravis, myocardial ischemia, obstructive uropathy, renal disease, severe ulcerative colitis, tachycardia, toxic megacolon, unstable cardiovascular status in acute hemorrhage

Interactions

adsorbent antidiarrheals, antacids: Decreased atropine absorption amantadine, anticholinergics, antidyskinetics, glutethimide, meperidine, muscle relaxants, phenothiazines, tricyclic antidepressants and other with anticholinergic properties, including antiarrhythmics (disopyramide, procainamide, quinidine), antihistamines, buclizine, meclizine: Increased atropine effects antimyasthenics: Reduced intestinal motility cyclopropane: Risk of ventricular arrhythmias
haloperidol: Decreased antipsychotic effect
ketoconazole: Decreased ketoconazole absorption metoclopramide: Decreased effect on GI motility opioid analgesics: Increased risk of ileus, severe constipation, and urine retention potassium chloride, especially wax-matrix for
MS: Possibly GI ulcers urinary alkalizers (calcium or magnesium antacids, carbonic anhydrase inhibitors, citrates, sodium bicarbonate): Delayed excretion,increased risk of adverse atropine effects

Side Efect

CNS: Agitation, amnesia, anxiety, ataxia, Babinski’s or Chaddock’s reflex, behavioral changes, CNS stimulation (at high doses), coma, confusion, decreased concentration, decreased tendon reflexes, delirium, dizziness, drowsiness, fever, hallucinations, headache, hyperreflexia, insomnia, lethargy, mania, mental disorders, nervousness, paranoia, restlessness, seizures, somnolence, stupor, syncope, vertigo, weakness
CV: Arrhythmias, bradycardia (at low doses), cardiac dilation, chest pain, hypertension, hypotension, left ventricular failure, MI, palpitations, tachycardia (at high doses), weak or impalpable peripheral pulses
EENT: Acute angle-closure glaucoma, altered taste, blepharitis, blindness, blurred vision, conjunctivitis, cyclophoria, cycloplegia, decreased visual acuity or accommodation, dry eyes or conjunctiva, dry mucous membranes, dry mouth, eye irritation, eyelid crusting, heterophoria, increased intraocular pressure, keratoconjunctivitis, lacrimation, laryngitis, laryngospasm, mydriasis, nasal congestion, oral lesions, photophobia, pupils poorly reactive to light, strabismus, tongue chewing
GI: Abdominal distention, abdominal pain, bloating, constipation, decreased bowel sounds or food absorption, delayed gastric emptying, dysphagia, heartburn, ileus, nausea, vomiting
GU: Bladder distention, enuresis, impotence, urinary hesitancy, urinary urgency, urine retention
MS: Dysarthria, hypertonia, muscle twitching
RESP: Bradypnea, dyspnea, inspiratory stridor, pulmonary edema, respiratory failure, shallow breathing, subcostal recession, tachypnea
SKIN: Cold skin, cyanosis, decreased sweating, dermatitis, flushing, rash, urticaria
Other: Anaphylaxis, dehydration, injection site reaction, polydipsia, sensations of warmth atropine 114

Cautions

WARNING For patient prescribed AtroPen for suspected nerve gas or insecticide exposure, dosage is determined by severity of symptoms. Mild symptoms include blurred vision, miosis, excessive unexplained teary eyes or runny nose, increased salivation, chest tightness, difficulty breathing, tremors, muscle twitching, nausea, vomiting, unexplained wheezing or coughing, acute onset of stomach cramps, tachycardia, and bradycardia. Severe symptoms include confusion or other strange behavior, severe difficulty breathing, extreme secretions from airway or lungs, severe muscle twitching and general weakness, involuntary urination and defecation, seizures, and unconsciousness.

Avoid using high-dose atropine sulfate in patients with ulcerative colitis because of risk of toxic megacolon or in patients with hiatal hernia and reflux esophagitis because of risk of esophagitis

AtroPen has no absolute contraindications when used to treat life-threatening nerve gas or insecticide exposure.
WARNING Assess for symptoms of toxic doses of atropine, such as excitement, agitation, drowsiness, and confusion, which are likely to affect elderly patients even with low doses. If symptoms occur, take safety precautions to prevent injury.

Assess bowel and bladder elimination. Notify prescriber of diarrhea, constipation, urinary hesitancy, or urine retention.

PATIENT SAFTY

For patient prescribed an AtroPen to carry because of risk of nerve gas or insecticide exposure, explain when and how to selfadminister the drug.

Instruct patient to take atropine sulfate 30 to 60 minutes before meals.

Advise patient to notify prescriber if he has persistent or severe diarrhea, constipation, or difficulty urinating.

Category

Chemical class: Gold salt
Therapeutic class: Anti-inflammatory

Pregnancy category: C

Indications

To treat active rheumatoid arthritis that’s unresponsive to NSAIDs
Adults. Initial: 6 mg daily or 3 mg b.i.d. Maintenance: Up to 9 mg daily after 3 mo of treatment, if needed. Children age 6 and over. Initial: 0.1 mg/kg daily. Maintenance: 0.15 mg/kg daily. Maximum: 0.2 mg/kg daily.
DOSAGE ADJUSTMENT Drug discontinued if therapeutic response isn’t adequate after 3 mo at 9 mg daily. Route Onset Peak Duration P.O. 3–6 mo 1–2 hr Up to 26 days

Mechanism of Action

Decreases rheumatoid factor and humoral antibody (immunoglobulin) levels. Although exact anti-inflammatory action is unknown, drug may suppress the increased phagocytic activity of macrophages and polymorphonuclear leukocytes that occurs with rheumatoid arthritis and thereby inhibit release of destructive enzymes that cause joint inflammation.

Contraindications

Agranulocytosis, blood dyscrasias, bone marrow aplasia, colitis, eczema, exfoliative dermatitis, hepatic disease, history of gold or heavy metal toxicity, hypersensitivity to auranofin, marked hypertension, necrotizing enterocolitis, pulmonary fibrosis, recent radiation therapy, renal disease, severe debilitation, systemic lupus erythematosus, uncontrolled diabetes mellitus, uncontrolled heart failure, urticaria, youth (under age 6)

Interactions

phenytoin: Possibly increased phenytoin level

Side Efect

CNS: Confusion, dizziness, EEG abnormalities, hallucinations, seizures
EENT: Gingivitis, glossitis, iritis or corneal ulcers from gold deposits in ocular tissue, metallic taste, stomatitis
GI: Abdominal cramps, anorexia, constipation, diarrhea, enterocolitis, flatulence, indigestion, melena, nausea, vomiting
GU: Hematuria, elevated BUN and serum creatinine levels, proteinuria, vaginitis
HEME: Agranulocytosis, aplastic anemia, eosinophilia, leukopenia, neutropenia, thrombocytopenia
RESP: Cough, dyspnea, fibrosis, interstitial pneumonitis
SKIN: Alopecia, dermatitis, exfoliative dermatitis, jaundice, photosensitivity, pruritus, rash, urticaria

Cautions

Monitor blood and urine tests for signs of gold toxicity during auranofin therapy.
WARNING Gold toxicity may occur during treatment or several months afterward. It usually occurs with a cumulative dose of 400 to 800 mg and may cause decreased hemoglobin level, WBC count less than 4,000/mm3, granulocyte count less than 1,500/mm3, platelet count less than 150,000/mm3, severe diarrhea, stomatitis, hematuria, proteinuria, rash, and pruritus.

Monitor fluid intake and output imbalance. If urine output decreases, assess BUN and serum creatinine levels for signs of renal impairment.

Notify prescriber about possible allergic reaction (dermatitis, rash, pruritus). Drug may need to be discontinued.

PATIENT SAFTY

vAdvise patient that diarrhea is common but that he should notify prescriber immediately if it becomes severe.

Tell patient to take drug exactly as prescribed and to have monthly blood tests.

Inform patient that drug may take 3 to 4 months to reach a therapeutic level.

Urge patient to report skin problems, fatigue, or stomatitis (possible blood dyscrasias).

Tell patient to report blood in stool or urine, easy bruising, and bleeding gums.

Category

Chemical class: Purine analogue
Therapeutic class: Antimetabolite, immunosuppressant

Pregnancy category: D

Indications

To prevent kidney rejection after transplantation ,
IV: Adults and children.Initial: 3 to 5 mg/kg daily P.O. or I.V. as a single dose on, or 1 to 3 days before, day of transplantation, followed by 3 to 5 mg/kg daily I.V. after surgery until P.O. dose is tolerated. Maintenance: 1 to 3 mg/kg daily P.O.
DOSAGE ADJUSTMENT Dosage reduced for patients with oliguria (as from tubular necrosis) after transplantation because drug or metabolite excretion may be delayed. To treat refractory rheumatoid arthritis
Adults. Initial: 1 mg/kg (50 to 100 mg) daily as a single dose or b.i.d. for 6 to 8 wk. Maintenance: If initial therapy doesn’t produce therapeutic effects or serious adverse effects, dosage increased every 4 wk by 0.5 mg/kg up to 2.5 mg/kg. Optimal dosage is 2 to 2.5 mg/kg daily.
DOSAGE ADJUSTMENT Dosage reduced to 25% to 33% of usual dosage for patients who also take allopurinol. Route Onset Peak Duration P.O., I.V. 4–8 wk Unknown Several days

Mechanism of Action

May prevent proliferation and differentiation of activated B and T cells by interfering with purine (protein) and nucleic acid (DNA and RNA) synthesis.

Contraindications

Hypersensitivity to azathioprine

Interactions

ACE inhibitors and that affect bone marrow and cell development in bone marrow, such as co-trimoxazole: Possibly severe leukopenia allopurinol: Possibly increased therapeutic and adverse effects of azathioprine anticoagulants: Possibly decreased anticoagulant action cyclosporine: Possibly decreased plasma azathioprine 116 cyclosporine level methotrexate: Possibly increased plasma level of azathioprine’s metabolite, 6-mercaptopurine, which can lead to cell death nondepolarizing neuromuscular blockers: Possibly decreased or reversed action of neuromuscular blocker

Side Efect

CNS: Fever, malaise
GI: Abdominal pain, diarrhea, hepatoxicity (elevated liver function test results), nausea, pancreatitis, steatorrhea, vomiting
HEME: Leukopenia, macrocytic anemia, pancytopenia, thrombocytopenia
MS: Arthralgia, myalgia
SKIN: Alopecia, rash
RESP: Reversible interstitial pneumonitis
Other: Infection, lymphomas and other neoplasms, negative nitrogen balance

Cautions

Before I.V. use, add 20 ml sterile water for injection to azathioprine vial and swirl until clear solution forms. Resulting drug concentration is 100 mg and can be diluted further as prescribed. Calculate infusion rate based on final volume to be infused. Then give over 30 to 60 minutes or as prescribed (5 minutes to 8 hours).

Obtain results of baseline laboratory tests, including WBC, RBC, and platelet counts. Expect to monitor results once a week during first month of therapy, twice a month during second and third months, and once a month or more thereafter.

Hematologic reactions typically are doserelated and may occur late in therapy, especially in patients with transplant rejection.
WARNING If WBC count decreases rapidly or remains significantly and consistently low, expect to reduce dosage or discontinue azathioprine.

Periodically monitor liver function test results for early signs of hepatotoxicity.

If patient develops thrombocytopenia, take bleeding precautions, such as avoiding I.M. injections and venipunctures, applying ice to areas of trauma, and checking I.V. infusion sites every 2 hours for bleeding.

If patient also receives an oral anticoagulant, monitor his PT.

Azathioprine therapy increases risk of viral, fungal, bacterial, and protozoal infections. Watch for evidence of infection, such as fever, chills, sore throat, and mouth sores. Expect to administer aggressive antibiotic, antiviral, or other drug therapy and reduce azathioprine dosage.

Minimize the risk of infection. If patient has severe leukopenia, take neutropenic precautions, such as placing him in a private room and limiting visitors.

Rheumatoid arthritis requires at least 12 weeks of azathioprine therapy. During this time, continue other pain-relief measures, such as rest, physical therapy, and other , such as salicylates and corticosteroids.

If oral azathioprine causes GI upset, give it in divided doses or with meals.

Expect to use lowest possible maintenance dosage for rheumatoid arthritis, reducing it gradually in 0.5-mg/kg (about 25-mg) increments at 4-week intervals.

Drug can be stopped abruptly, but its effects may persist several days.

PATIENT SAFTY

Advise patient to take oral drug with food or meals to minimize GI upset.
WARNING Teach patient to recognize and report signs of infection, such as sore throat and fever.

Teach patient how to reduce the risk of bleeding and falling.

Category

Chemical class: Phthalazinone derivative
Therapeutic class: Antihistamine, H1-receptor antagonist

Pregnancy category: C

Indications

To treat symptoms of seasonal rhinitis (rhinorrhea, sneezing, and nasal itching)
NASAL SPRAY Adults and children age 12 and over. 2 sprays in each nostril b.i.d.

Mechanism of Action

Binds nonselectively to central and peripheral H1receptors, preventing histamine from reaching its site of action, which reduces or prevents most of histamine’s physiologic effects. By blocking histamine at its site of action, azelastine inhibits respiratory, vascular, and GI smooth-muscle contraction; decreases capillary permeability, which reduces wheals, flares, and itching; and decreases salivary and lacrimal gland secretions. Route Onset Peak Duration Nasal In 3 hr Unknown 12 hr

Contraindications

Hypersensitivity to azelastine or its components

Interactions

cimetidine,
ketoconazole: Possibly increased blood azelastine level
CNS depressants: Possibly increased sedative effects and reduced mental alertness
alcohol use: Possibly increased sedative effects and reduced mental alertness

Side Efect

CNS: Dizziness, fatigue, headache, somnolence
CV: Atrial fibrillation, palpitations
EENT: Bitter taste, dry mouth, epistaxis, nasal burning, paroxysmal sneezing, pharyngitis, rhinitis
GI: Nausea
Other: Weight gain

Cautions

Assess for changes in alertness, and take safety precautions, if needed.

PATIENT SAFTY

Teach patient how to use azelastine nasal spray properly to achieve maximum therapeutic effects.

Before patient’s first use of
NASAL SPRAY, instruct him to prime pump by placing his thumb on base and his index and middle fingers on shoulder area of bottle and then pressing thumb firmly and quickly against bottle four times or until fine mist appears.

If patient hasn’t used spray in more than 3 days, instruct him to reprime pump with two sprays or until fine mist appears.

Advise patient to clear nostrils gently, if needed, before using spray.

Teach patient to inhale deeply after each spray and then exhale through his mouth and tilt his head back so drug can spread over nasopharynx.

Advise patient to store bottle upright and tightly closed.
WARNING Emphasize that patient must consult prescriber before taking any OTC drug, such as cough syrup or a cold remedy, because of the risk of extreme CNS depression.

Inform patient that decreased alertness may occur. Advise him to avoid hazardous activities or those that require alertness, such as driving or operating machinery, until drug’s effects are known.

Category

Chemical class: Azalide (subclass of macrolide)
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat mild community-acquired pneumonia, otitis media, pharyngitis, tonsillitis, and uncomplicated skin and soft-tissue infections , ORAL SUSPENSION,
Adults.500 mg as a single dose on day 1, followed by 250 mg daily on days 2 through 5. Children age 6 months or over with acute otitis media or community-acquired pneumonia.10 mg/kg as a single dose (not to exceed 500 mg daily) on day 1, followed by 5 mg/kg (not to exceed 250 mg daily) daily on days 2 through 5. Or, for acute otitis media, 30 mg/kg of oral suspension as a single dose or 10 mg/kg daily for 3 days. Children age 12 or over with pharyngitis or tonsillitis.12 mg/kg (not to exceed 500 mg daily) as single dose daily for 5 days. To treat mild to moderate acute bacterial exacerbations of COPD , ORAL SUSPENSION,
Adults. 500 mg daily for 3 days. Or, 500 mg as single dose on day 1, followed by 250 mg azithromycin 118 daily on days 2 through 5. To treat community-acquired pneumonia , ORAL SUSPENSION,, I.V. INFUSION Adults and adolescents age 16 or over. 500 mg I.V. as a single dose daily for at least 2 days, followed by 500 mg P.O. as a single dose daily until patient completes 7 to 10 days of therapy. To treat community-acquired pneumonia caused by Chlamydophila pneumoniae, Haemophilus influenzae, Mycoplasma pneumoniae, or Streptococcus pneumoniae (ZMAX)
Adults. 2 g as a single dose on an empty stomach. To treat chancroid caused by Haemophilus ducreyi; gonococcal pharyngitis; urethritis, cervicitis, or other infections caused by Chlamydia trachomatis , ORAL SUSPENSION,
Adults. 1 g as a one-time dose. Children age 8 or over and children under age 8 weighing 45 kg (99 lb) or more (with infections caused by C. trachomatis). 1 g as a one-time dose. To treat urethritis or cervicitis caused by Neisseria gonorrhoeae , ORAL SUSPENSION,
Adults.2 g as a one-time dose. To prevent Mycobacterium avium complex in patients with advanced HIV infection , ORAL SUSPENSION,, I.V. INFUSION
Adults.1.2 g once weekly, as indicated. To treat pelvic inflammatory disease , ORAL SUSPENSION,, I.V. INFUSION
Adults.500 mg I.V. as a single dose daily for 1 to 2 days, followed by 250 mg P.O. as a single dose daily until patient completes 7 days of therapy. To treat acute bacterial sinusitis ORAL SUSPENSION,
Adults. 500 mg daily for 3 days. Children.10 mg/kg daily for 3 days. To treat acute bacterial sinusitis caused by H. influenzae, Moraxella catarrhalis, or S. pneumoniae

ORALL

(ZMAX)
Adults.2 g as a single dose on an empty stomach. Route Onset Peak Duration P.O. Varies Unknown Unknown

Mechanism of Action

Binds to a ribosomal subunit of susceptible bacteria, blocking peptide translocation and inhibiting RNA-dependent protein synthesis. Drug concentrates in phagocytes, macrophages, and fibroblasts, which release it slowly and may help move it to infection sites.

Incompatibilities

Don’t add I.V. substances, additives, or to azithromycin I.V. solution, and don’t infuse through the same I.V. line.

Contraindications

Hypersensitivity to azithromycin, erythromycin, ketolide antibiotics, or other macrolide antibiotics

Interactions

antacids that contain aluminum or magnesium: Possibly decreased peak blood azithromycin level, but extent of absorption is unchanged carbamazepine, cyclosporine, phenytoin, terfenadine ( metabolized by P-450 cytochrome system): Possibly increased blood levels of these digoxin: Possibly increased blood digoxin level dihydroergotamine, ergotamine: Possibly severe peripheral vasospasm and abnormal sensations (acute ergot toxicity) HMG-CoA reductase inhibitors: Increased risk of severe myopathy or rhabdomyolysis pimozide: Possibly sudden death oral anticoagulants: Possibly potentiated effects of oral anticiagulants
theophylline: Possibly increased blood theophylline level triazolam: Possibly decreased excretion and increased therapeutic effects of triazolam
warfarin: Possibly increased anticoagulation food: Dramatically increased absorption rate of azithromycin

Side Efect

CNS: Aggressiveness, agitation, anxiety, asthenia, dizziness, fatigue, headache, hyperactivity, malaise, nervousness, paresthesia, seizures, somnolence, syncope, vertigo
CV: Chest pain, edema, elevated serum CK level, hypotension, palpitations, prolonged QT interval, torsades de pointes, ventricular tachycardia
EENT: Hearing loss, mucocutaneous candidiasis, perversion or loss of taste or smell, tinnitus
ENDO: Hyperglycemia
GI: Abdominal pain, anorexia, cholestatic jaundice, constipation, diarrhea, dyspepsia, elevated liver function test results, flatulence, hepatic necrosis or failure, hepatitis, nausea, pancreatitis, pseudomembranous colitis, vomiting
GU: Acute renal failure, elevated BUN and serum creatinine levels, nephritis, vaginal candidiasis
HEME: Leukopenia, neutropenia, thrombocytopenia
MS: Arthralgia
SKIN: Erythema multiforme, photosensitivity, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Allergic reaction, anaphylaxis, angioedema, elevated serum phosphorus level, hyperkalemia, infusion site reaction (such as pain and redness), new or worsening myasthenia syndrome, superinfection

Cautions

Obtain culture and sensitivity test results, if possible, before starting therapy.

Use azithromycin cautiously in patients with hepatic dysfunction (drug is metabolized in the liver) or renal dysfunction (effects are unknown in this group).

Give azithromycin capsules 1 hour before or 2 to 3 hours after food. Give tablets or suspension without regard to food.
WARNING Don’t give azithromycin by I.V. bolus or I.M. injection because it may cause erythema, pain, swelling, tenderness, or other reaction at the site. Infuse it over 60 minutes or longer, as prescribed (typically 1 mg/ml over 3 hours or 2 mg/ml over 1 hour.)

If hepatic function is impaired, monitor liver function studies because drug is eliminated mainly by the liver.

Assess patient for bacterial or fungal superinfection, which may occur with prolonged or repeated therapy. If it occurs, expect to give another antibiotic or antifungal.

Monitor bowel elimination; if needed, obtain stool culture to rule out pseudomembranous colitis. If it occurs, expect to stop azithromycin and give fluid, electrolytes, and antibiotics effective with Clostridium difficile.

PATIENT SAFTY

Tell patient to take azithromycin capsules 1 hour before or 2 to 3 hours after food. Instruct patient to take tablets or suspension without regard to food.
WARNING Urge patient to consult prescriber before taking OTC , including antacids. If they’re prescribed, tell patient to take azithromycin 1 hour before or 2 to 3 hours after taking antacids.

Tell patient to immediately report signs and symptoms of allergic reaction (such as rash, itching, hives, chest tightness, and trouble breathing).

Warn patient that abdominal pain and loose, watery stools may occur. If diarrhea persists or becomes severe, urge him to contact prescriber and replace fluids.

Because azithromycin may destroy normal flora, teach patient to watch for and immediately report signs of superinfection, such as white patches in the mouth.

Category

Chemical class: Monobactam
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat infections of the urinary tract, lower respiratory tract, skin, soft tissue, female reproductive tract; intra-abdominal infections; septicemia; and surgical abscesses caused by susceptible strains of gram-negative bacteria
IV:, I.V.OR
I.M.INJECTION
Adults.0.5 to 2 g every 8 to 12 hr to maximum of 8 g daily. For life-threatening systemic infection, 2 g every 6 to 8 hr to maximum of 8 g daily. Children ages 9 months to 16 years. 30 mg/kg every 6 to 8 hr up to 120 mg/kg aztreonam 120 daily; 50 mg/kg every 4 to 6 hr (for Pseudomonas aeruginosa).
DOSAGE ADJUSTMENT If creatinine clearance is 10 to 30 ml/min/1.73 m2, initial dose is 1 to 2 g; then 50% of usual dose at usual interval. If creatinine clearance is less than 10 ml/ min/1.73 m2, initial dose is 500 mg to 2 g; then 25% of the usual dose every 6, 8, or 12 hr. Route Onset Peak Duration I.V. Immediate Immediate Unknown infusion I.V. Immediate Immediate Unknown injection I.M. Variable 60 min Unknown

Mechanism of Action

Inhibits bacterial cell wall synthesis in susceptible aerobic gram-negative bacteria. These bacteria assemble rigid, cross-linked cell walls in several steps. Aztreonam affects the final cross-linking step by inactivating penicillin-binding protein 3 (the enzyme that links cell wall strands), which causes cell lysis and death.

Incompatibilities

Don’t mix aztreonam in same I.V. solution as cephradine, metronidazole, or nafcillin sodium. Don’t mix it in same I.M. injection solution as local anesthetic.

Contraindications

Hypersensitivity to aztreonam or its components

Interactions

aminoglycosides (prolonged or high-dose therapy): Increased risk of nephrotoxicity and ototoxicity cefoxitin, imipenem: Possibly antagonized action of aztreonam furosemide, probenecid: Possibly increased blood aztreonam level

Side Efect

CNS: Confusion, dizziness, fever, headache, insomnia, malaise, paresthesia, seizures, vertigo
CV: Chest pain, hypotension, transient ECG changes
EENT: Altered taste, diplopia, halitosis, mouth ulcers, mucocutaneous candidiasis, nasal congestion, sneezing, tinnitus, tongue numbness
GI: Abdominal cramps, diarrhea, elevated liver function test results, GI bleeding, hepatitis, nausea, pseudomembranous colitis, vomiting
GU: Breast tenderness, elevated serum creatinine level, vaginal candidiasis
HEME: Anemia, eosinophilia, leukocytosis, neutropenia, pancytopenia, positive Coombs’ test, prolonged PT and APTT, thrombocytopenia, thrombocytosis
MS: Myalgia
RESP: Bronchospasm, dyspnea, wheezing
SKIN: Diaphoresis, erythema multiforme, exfoliative dermatitis, flushing, jaundice, petechiae, pruritus, purpura, rash, toxic epidermal necrolysis, urticaria
Other: Allergic reaction; injection site pain, phlebitis, swelling, or thrombophlebitis

Cautions

Obtain culture and sensitivity test results, if possible, before starting aztreonam therapy. If patient is acutely ill, expect to begin therapy before results are available.

Keep in mind that other antimicrobials may be used with aztreonam in seriously ill patients at risk for gram-positive infection.

Expect to use I.V. route for patients who need single doses over 1 g and those with life-threatening systemic infections, such as septicemia or peritonitis.

To reconstitute aztreonam for I.V. bolus injection, use sterile water for injection.

Immediately after adding diluent to vial, shake it vigorously to mix. After obtaining correct dose, discard unused solution.

Reconstituted solution may turn light pink on standing at room temperature. This doesn’t affect drug potency.

Give I.V. bolus injection directly into I.V. tubing over 3 to 5 minutes.
WARNING When preparing aztreonam for I.V. infusion, use at least 50 ml of appropriate infusion solution per gram of aztreonam. Further dilute drug in I.V. solution, such as normal saline solution, D5W, dextrose 5% in normal saline solution, lactated Ringer’s solution, or Ringer’s solution.

Know that I.V. infusion may be administered over 20 to 60 minutes.

Flush I.V. tubing with solution, such as normal saline solution, before and after administering I.V. infusion to reduce risk of incompatibilities.

If prescribed, mix aztreonam in same I.V. solution with other antibiotics (such as ampicillin sodium, cefazolin sodium, clindamycin phosphate, gentamicin sulfate, or tobramycin sulfate), or mix it with cloxacillin sodium and vancomycin hydrochloride in peritoneal dialysis solution.

Prepare solution for I.M. injection using sterile or bacteriostatic water or sodium chloride for injection. Administer injection deep into large muscle, such as in dorsogluteal or ventrogluteal area.

Assess for signs of bacterial or fungal superinfection, which may occur with prolonged or repeated therapy. If superinfection occurs, treat it as prescribed.

Monitor bowel elimination; if needed, obtain stool culture to rule out pseudomembranous colitis. If it occurs, expect to discontinue aztreonam and administer fluid, electrolytes, and antibiotics effective against Clostridium difficile.

Evaluate patient’s renal and liver function test results, as ordered, if patient has renal or hepatic impairment.

Monitor renal function if patient is receiving an aminoglycoside because of the increased risk of nephrotoxicity.

PATIENT SAFTY

Stress the need to take full course of aztreonam exactly as prescribed, even if patient feels better before finishing it.

Teach patient to recognize and immediately report signs and symptoms of allergic reactions, such as chest tightness, difficulty breathing, hives, itching, and rash.

Warn patient that abdominal pain and loose, watery stools may occur 2 months or more after aztreonam therapy stops. If diarrhea persists or becomes severe, urge him to contact prescriber and replace fluids.

Because aztreonam may destroy normal flora, teach patient to watch for and immediately report signs of superinfection, such as white patches in mouth.

Category

Chemical class: Aminopenicillin
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat upper respiratory tract infections (including otitis media) caused by streptococci, pneumococci, non–penicillinase-producing staphylococci, and Haemophilus influenzae; UTI caused by Escherichia coli, Proteus mirabilis, or Streptococcus faecalis; skin and softtissue infections caused by streptococci and susceptible staphylococci
Adults.400 mg every 12 hr; 800 mg every 12 hr for severe infections and those caused by less susceptible organisms. Children weighing 25 kg (55 lb) or more. 25 mg/kg daily in divided doses every 12 hr; 50 mg/kg daily in divided doses every 12 hr for severe infections and those caused by less susceptible organisms. To treat lower respiratory tract infections caused by streptococci, pneumococci, non–penicillinase-producing staphylococci, and H. influenzae
Adults. 800 mg every 12 hr. Children weighing 25 kg or more. 50 mg/ kg/day in divided doses every 12 hr. To treat uncomplicated gonorrhea caused by Neisseria gonorrhoeae
Adults. 1.6 g plus 1 g of probenecid as a single dose. Route Onset Peak Duration P.O. Variable Unknown 12 hr

Mechanism of Action

Inhibits bacterial cell wall synthesis in susceptible bacteria. These bacteria assemble rigid, cross-linked cell walls in several steps. Bacampicillin, which undergoes hydrolysis to ampicillin, affects final stage of crosslinking by binding with and inactivating penicillin-binding protein (enzyme responsible for linking cell wall strands). This action inhibits bacterial cell wall synthesis and causes cell lysis and death.

Contraindications

Cholestatic jaundice and hepatic dysfunction associated with amoxicillin and clavulanate potassium; hypersensitivity to penicillins, cephalosporins, imipenem and cilastatin, or beta-lactamase inhibitors, such as piperacillin and tazobactam

Interactions

allopurinol: Increased risk of rash from bacampicillin use beta-adrenergic blockers: Increased risk of anaphylaxis disulfiram: Possibly disulfiram reaction when administered together oral contraceptives: Possibly reduced effectiveness of oral contraceptives, contraceptive failure, and breakthrough bleeding tetracyclines: Possibly impaired bactericidal effects of bacampicillin

Side Efect

CNS: Anxiety, confusion, depression, fatigue, fever, hallucinations, lethargy, malaise, neuromuscular irritability, seizures, stroke, syncope
CV: Hypotension, palpitations, periarteritis nodosa, pulmonary hypertension, tachycardia, vascular collapse
EENT: Altered taste, black “hairy”tongue, blurred vision, glossitis, laryngospasm, mouth soreness, mucocutaneous candidiasis, stomatitis, taste disorders
GI: Abdominal cramps or pain, anorexia, diarrhea, enterocolitis, epigastric distress, elevated liver function test results, gastritis, nausea, pseudomembranous colitis, vomiting
GU: Elevated BUN and serum creatinine levels, hematuria, impotence, interstitial nephritis, neurogenic bladder, priapism, renal failure, vaginal candidiasis
HEME: Agranulocytosis, anemia, bone marrow depression, decreased hemoglobin level and hematocrit, eosinophilia, leukopeB nia, neutropenia, prolonged PT, thrombocytopenia, thrombocytopenic purpura
MS: Arthralgia, arthritis exacerbation
RESP: Bronchospasm
SKIN: Exfoliative dermatitis, rash, urticaria
Other: Allergic reaction, lymphadenopathy, serum sickness

Cautions

Obtain culture and sensitivity test results, if possible, before starting therapy. Expect to start drug before results are available.

Expect to continue treatment for at least 48 hours after symptoms resolve or culture detects no signs of infection.
WARNING Expect to give bacampicillin for 10 days to treat infection caused by group A beta-hemolytic streptococci to prevent development of acute rheumatic fever or acute glomerulonephritis.

Assess patient for bacterial or fungal superinfection, which may occur with prolonged or repeated therapy. If it occurs, expect to administer another antibiotic or antifungal drug.

Monitor bowel elimination; if needed, obtain stool culture to rule out pseudomembranous colitis. If this adverse reaction occurs, expect to discontinue bacampicillin and give fluid, electrolytes, and antibiotics effective against Clostridium difficile.

PATIENT SAFTY

Teach patient to recognize and immediately report signs of allergic reaction, including rash, itching, hives, chest tightness, and difficulty breathing.

Warn that abdominal pain and loose, watery stools may occur. If diarrhea persists or becomes severe, urge him to contact prescriber and drink plenty of fluids.

Because bacampicillin may destroy normal flora, teach patient to watch for and immediately report signs of superinfection, such as white patches in mouth and vaginal itching and discharge.

Category

Chemical class: Bacillus subtilis derivative (polypeptide)
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To treat pneumonia and empyema caused by susceptible staphylococci
I.M.INJECTION Infants weighing more than 2.5 kg (5.5 lb). 1,000 units/kg daily in 2 or 3 divided doses. Infants weighing less than 2.5 kg. 900 units/ kg daily in 2 or 3 divided doses. Route Onset Peak Duration I.M. Rapid Unknown About 6 hr

Mechanism of Action

Interferes with bacterial cell wall synthesis by binding with isoprenyl pyrophosphate (a lipid-carrying molecule that transports substances out of bacterial cells to help build new cell walls), forming an unusable complex in bacterial cells. This weakens cell walls and causes lysis and death. Bacitracin is considered bacteriostatic and bactericidal.

Incompatibilities

Don’t dilute bacitracin with a solution that contains parabens.

Contraindications

Hypersensitivity or toxic reaction to bacitracin

Interactions

aminoglycosides: Increased risk of respiratory paralysis and renal dysfunction nondepolarizing neuromuscular blockers: Possibly increased neuromuscular blockade

Side Efect

GI: Nausea, vomiting
GU: Albuminuria, azotemia, cylindrical mucus casts in urine, nephrotoxicity
SKIN: Rash
Other: Injection site pain, superinfection

Cautions

Obtain culture and sensitivity test results before therapy begins, if possible. Be prepared to start bacitracin therapy before results are available.
WARNING Use parenteral bacitracin for I.M. injection only.

For I.M. solution of 5,000 units/ml, reconstitute 50,000 units bacitracin powder with 9.8 ml sodium chloride for injection bacitracin 124 that contains 2% procaine hydrochloride.

Administer I.M. injection into upper outer quadrant of buttocks, alternating between right and left sides. To prevent pain at injection site, avoid giving multiple injections in same site.

During therapy, compare daily results of renal function tests with baseline results, as appropriate.

Assess urine output often (hourly, if needed), and replace fluids orally and parenterally to maintain adequate renal function.
WARNING Because of increased risk of nephrotoxicity, avoid concurrent use of other nephrotoxic , such as streptomycin, kanamycin, polymyxin B, and neomycin.

Assess infant for signs of superinfection, especially white patches in mouth and perineum. If superinfection develops, plan to treat with appropriate antibiotics.

PATIENT SAFTY

Advise parents that daily blood tests are needed to assess infant’s renal function.

Encourage parents to provide oral fluids to promote renal function. Teach them how to record infant’s fluid intake.

Instruct parents to report signs or symptoms of superinfection, such as white patches in mouth or perineal area and bright red diaper rash.

Category

Chemical class: Gamma-aminobutyric acid (GABA) chlorophenyl derivative
Therapeutic class: Skeletal muscle relaxant, spasmolytic

Pregnancy category: C

Indications

To relieve symptoms of spasticity caused by multiple sclerosis (particularly flexor spasms and pain, clonus, and muscle rigidity) and spasticity from spinal cord injury or disease and brain injury Adults and children age 12 and over. 5 mg t.i.d. for 3 days; then 10 mg t.i.d. for 3 days; then 15 mg t.i.d. for 3 days; then 20 mg t.i.d. for 3 days; then increased if needed up to 80 mg daily. Usual dosage ranges from 40 to 80 mg daily. To relieve severe symptoms of spasticity of spinal cord origin when symptoms don’t respond to oral drug or when oral drug causes severe adverse CNS effects

INTRATHECAL

BOLUS,

INTRATHECAL

INFUSION
Adults. For screening before implantable pump insertion: 50 mcg in 1 ml sterile preservative-free sodium chloride for injection as bolus injection into intrathecal space over 1 min or more. After 4 to 8 hr, if symptoms don’t improve as much as desired, second bolus of 75 mcg in 1.5 ml of sterile preservative-free sodium chloride for injection, injected after 24 hr, followed by third bolus of 100-mcg/2 ml dilution injected after another 24 hr, if needed. After implantable pump insertion: Effective screening dose doubled and infused over 24 hr. Or effective screening dose (if it provided desired effects for more than 12 hr) infused over 24 hr. For spasticity of spinal cord origin after implantable pump insertion: After first 24 hr, daily dose increased by 10% to 30% once every 24 hr until desired effects achieved. For spasticity of cerebral origin after implantable pump insertion: Daily dose increased by 5% to 15% once every 24 hr until desired effects achieved. For long-term maintenance therapy in spasticity of spinal cord origin: 12 to 2,003 mcg/ day (usual dose 300 to 800 mcg daily). Lowest possible therapeutic dose should be used. If adverse effects occur, daily dose may be decreased by 10% to 20%. During periodic pump refills, daily dose may be increased by 10% up to 40% to control symptoms adequately. For long-term maintenance therapy in spasticity of cerebral origin: 90 to 703 mcg daily (usual) but ranging from 22 to 1,400 mcg/ day. If adverse effects occur, daily dose may be decreased by 10% to 20%. During periodic pump refills, daily dose may be increased by 5% to 20% to control symptoms adequately. Children. For screening before implantable pump insertion: 1 ml of 50-mcg/ml dilution or 1 ml of 25-mcg/ml dilution (if child is very young) as bolus injection into intrathecal space over 1 min or more. After 4 to 8 hr, if symptoms don’t improve as desired, second bolus of 75 mcg in 1.5 ml of sterile preservative-free sodium chloride for injection, injected after 24 hr, followed by third bolus of 100-mcg/2 ml dilution, injected after another 24 hr, if needed. After implantable pump insertion: Daily dose increased by 5% to 15% once every 24 hr until desired effect is achieved. For maintenance therapy: In children over age 12—90 to 703 mcg daily (usual), ranging from 22 to 1,400 mcg daily. In children under age 12—274 mcg daily (average), ranging from 24 to 1,199 mcg daily.
DOSAGE ADJUSTMENT Dosage reduced for patients with renal impairment because drug is excreted primarily unchanged by kidneys. Route Onset Peak Duration P.O. Hours– Unknown Unknown weeks Intrathecal 30–60 About 4–8 hr bolus min 4 hr injection Intrathecal 6–8 hr 24–48 hr Unknown infusion

Mechanism of Action

May inhibit transmission of monosynaptic and polysynaptic impulses, similar to effects of gamma-aminobutyric acid (GABA). Baclofen may work in the spinal cord at the afferent spinal end of upper motor neurons, where it hyperpolarizes nerve fibers and inhibits impulse transmission. This reduces excess muscle activity caused by muscle hypertonia, spasms, and spasticity.

Contraindications

Hypersensitivity to baclofen; treatment of skeletal muscle spasm resulting from rheumatic disorders, cerebral palsy, Parkinson’s disease, or stroke (oral form only)

Interactions

CNS depressants: Possibly increased CNS depression epidural morphine: Possibly hypotension and dyspnea
alcohol use: Possibly increased CNS depression

Side Efect

CNS: Abnormal gait, anxiety, ataxia, chills, coma, confusion, depression, dizziness, drowsiness, dystonia, emotional lability, euphoria, excitement, fatigue, fever, hallucinations, headache, hypertonia, hypothermia, hypotonia, impaired concentration, insomnia, lack of coordination, lethargy, memory loss, paresthesia, personality disorder, seizures, somnolence, stroke, syncope, tremor, weakness
CV: Bradycardia, chest pain, chest tightness, deep vein thrombosis, hypertension, orthostatic hypotension, palpitations, peripheral edema
EENT: Amblyopia, blurred vision, diplopia, dry mouth, miosis, mydriasis, nasal congestion, nystagmus, photophobia, ptosis, rhinitis, slurred speech, strabismus, taste loss, tinnitus
ENDO: Hyperglycemia
GI: Abdominal pain, anorexia, constipation, dysphagia, elevated liver function test results, flatulence, ileus, indigestion, nausea, vomiting
GU: Albuminuria, bladder spasms, dysuria, enuresis, hematuria, impotence, renal failure, sexual dysfunction, urinary frequency, urinary incontinence, urine retention
HEME: Anemia
MS: Muscle twitching
RESP: Aspiration pneumonia, pulmonary embolism, respiratory depression
SKIN: Alopecia, diaphoresis, facial edema, flushing, pruritus, rash, urticaria, wound dehiscence
Other: Dehydration, infection at pump implantation site, weight loss

Cautions

Expect to start baclofen therapy at a low dose and gradually increase until desired effects are achieved.
WARNING Before screening dose is given, expect prescriber to make sure patient is free of infection to prevent systemic infection from interfering with patient’s response. Before implantable pump insertion, also expect prescriber to make sure patient is free of infection to reduce risk of complications and interference with determining most appropriate dose.

Use baclofen cautiously in patients with a history of autonomic dysreflexia. Nociceptor stimulation may precipitate baclofen 126 autonomic dysreflexia. Be aware that abrupt withdrawal of intrathecal infusion may produce symptoms similar to autonomic dysreflexia, high fever, life-threatening complications such as multiple organsystem failure, and death.
WARNING Never give intrathecal form of baclofen by I.V., I.M., or subcutaneous routes.

Assess for signs of effectiveness, such as relief of spasms, pain, and muscle rigidity.

Because CNS depression can occur, take precautions to prevent injury. Also take precautions for patients who use spasticity to maintain locomotion or upright posture and balance. Relief of spasticity may increase risk of falls and injury.
WARNING Because continuous intrathecal infusion increases risk of life-threatening CNS depression, keep emergency equipment nearby.

Expect baclofen to be discontinued slowly; hallucinations and seizures may occur with abrupt withdrawal.

PATIENT SAFTY

Teach patient how to care for and operate programmable implanted pump. Have her demonstrate all procedures.

Advise against stopping baclofen abruptly. Stress the importance of keeping followup appointments for intrathecal infusion.

Instruct patient to avoid driving and other activities that require mental alertness, coordination, or physical dexterity until baclofen’s effects are known.

Urge patient to contact prescriber before taking OTC , such as cough syrups and cold remedies, which may increase risk of sedation.

Urge patient to notify prescriber if spasticity increases or drug is no longer effective.

Category

Chemical class: Prodrug of 5-aminosalicylic acid (5-ASA)
Therapeutic class: Anti-inflammatory

Pregnancy category: B

Indications

To treat mildly to moderately active ulcerative colitis
Adults.2.25 g t.i.d. for 8 wk. Maximum: 6.75 g daily for 12 wk. Children ages 5 to 17. 750 mg or 2.25 g t.i.d. for up to 8 wk.

Mechanism of Action

After it has been metabolized to 5-ASA, balsalazide may reduce inflammation by inhibiting the enzyme cyclooxygenase and decreasing production of arachidonic acid metabolites, which may be increased in patients with inflammatory bowel disease. Cyclooxygenase is needed to form prostaglandin from arachidonic acid. Prostaglandin mediates inflammatory activity and produces signs and symptoms of inflammation. By inhibiting prostaglandin synthesis, balsalazide may reduce signs and symptoms of inflammation in inflammatory bowel disease. Balsalazide also interferes with leukotrine synthesis and inhibits the enzyme lipoxygenase. These substances are involved in the inflammatory response.

Contraindications

Hypersensitivity to balsalazide, salicylates, or their components

Side Efect

CNS: Fatigue, fever, headache, insomnia
CV: Myocarditis, pericarditis, vasculitis
EENT: Dry mouth, nasopharyngitis, pharyngitis, rhinitis, stomatitis
GI: Abdominal cramps or pain, anorexia, cirrhosis, constipation, diarrhea, dyspepsia, elevated liver enzyme levels, exacerbation of colitis, flatulence, hepatotoxicity, jaundice, nausea, pancreatitis, vomiting
GU: Dysmenorrhea, interstitial nephritis, renal failure, UTI
MS: Arthralgia, myalgia
RESP: Alveolitis, cough, flulike syndrome, pleural effusion, pneumonia, respiratory tract infection
SKIN: Alopecia, pruritus

Cautions

WARNING Monitor patients who are sensitive to sulfasalazine or olsalazine for possible cross-sensitivity to balsalazide.

Monitor patients with pyloric stenosis for balsalazide disodium 127 B decreased or delayed drug effects due to prolonged gastric retention of balsalazide capsules.

Monitor patient for possible exacerbation of colitis symptoms.

PATIENT SAFTY

Inform patient that balsalazide is used to reduce bowel inflammation and pain in ulcerative colitis and to minimize recurring inflammation.

Instruct patient to swallow capsules whole, with a full glass of water, and not to crush or chew them.

Advise patient to notify prescriber of any other she may be taking, including OTC , nutritional supplements, and herbal products, because they may interact with balsalazide.

Instruct patient to notify prescriber immediately if colitis symptoms worsen.

Inform patient that she can expect some improvement in symptoms in 3 to 21 days but that optimal results may take up to 6 weeks of treatment.

Category

Chemical class: Chimeric (murine or human) monoclonal antibody
Therapeutic class: Immunosuppressant

Pregnancy category: B

Indications

To prevent acute rejection in kidney transplantation

IV

OR INJECTION Adults and adolescents over age 15. 20 mg within 2 hr before transplantation; then 20 mg 4 days after transplantation. Children and adolescents ages 2 to 15. 12 mg/m2within 2 hr before transplantation; then 12 mg/m24 days after transplantation. Maximum: 20 mg/dose. Route Onset Peak Duration I.V. Unknown Unknown 22–50 days

Mechanism of Action

Initiates immunosuppression by blocking interleukin-2 receptors located on the surface of activated T cells. Normally, interleukin-2 is released by stimulated T lymphocytes, causing activation and differentiation of other T lymphocytes responsible for cell-mediated immunity.

Incompatibilities

Don’t add or infuse any other simultaneously through same I.V. line.

Contraindications

Hypersensitivity to basiliximab or its components

Side Efect

CNS: Asthenia, dizziness, fever, headache, insomnia, tremor
CV: Hypertension, peripheral edema
EENT: Oral candidiasis, pharyngitis, rhinitis
ENDO: Hyperglycemia
GI: Abdominal pain, constipation, diarrhea, indigestion, nausea, vomiting
GU: Dysuria, increased urinary nitrogen level, UTI
HEME: Anemia
MS: Back pain, leg pain
RESP: Cough, dyspnea, upper respiratory tract infection
SKIN: Acne
Other: Hypercholesterolemia, hyperkalemia, hyperuricemia, hypocalcemia, hypokalemia, hypophosphatemia, impaired wound healing, injection site reaction, metabolic acidosis, weight gain

Cautions

To reconstitute basiliximab, add 5 ml sterile water for injection to powder and shake vial gently to dissolve. Further dilute with normal saline solution or D5W for infusion to a volume of 50 ml. Gently invert infusion bag to avoid foaming; don’t shake. Drug should appear clear to opalescent and colorless.

Give reconstituted drug I.V. over 20 to 30 minutes or as bolus dose directly through central or peripheral I.V. line. Be aware that bolus dose may cause nausea, vomiting, and a localized injection-site reaction, including pain.

Expect drug to be given as adjunct to cyclosporine and corticosteroids.

Don’t store drug at room temperature for longer than 4 hours; don’t refrigerate for longer than 24 hours. basiliximab 128
WARNING Patient may develop hypersensitivity reactions (anaphylaxis, bronchospasm, dyspnea, hypotension, pruritus, rash, respiratory failure, sneezing, tachycardia, urticaria, wheezing) on initial exposure or following re-exposure after several months. Notify prescriber immediately if such reactions occur.

PATIENT SAFTY

Inform patient that second dose of basiliximab will be given 4 days after transplantation and that she may also receive cyclosporine and corticosteroid therapy.

Inform patient that because of drug’s immunosuppressant effects, she may experience slower wound healing and be more susceptible to upper respiratory tract infections.

Category

Chemical class: Synthetic glucocorticoid
Therapeutic class: Antiasthmatic, antiinflammatory

Pregnancy category: C

Indications

To control and prevent symptoms in patients with chronic asthma and those who also require oral corticosteroids INHALATION AEROSOL (84 MCG) Adults and children age 12 and over. Initial: 2 inhalations (168 mcg) b.i.d. For patients with severe asthma, 6 to 8 inhalations (504 to 672 mcg) daily with dosage reduced based on patient response. Maximum: 10 inhalations (840 mcg) daily. Children ages 6 to 12. Initial: 2 inhalations (168 mcg) b.i.d. Maximum: 5 inhalations (420 mcg) daily. INHALATION AEROSOL (42 MCG) Adults and children age 12 and over. Initial: 2 inhalations (84 mcg) t.i.d. or q.i.d. or 4 inhalations (168 mcg) b.i.d. For patients with severe asthma, 12 to 16 inhalations (504 to 672 mcg) daily with dosage reduced based on patient response. Maximum: 20 inhalations (840 mcg) daily. Children ages 6 to 12. Initial: 1 or 2 inhalations (42 mcg or 84 mcg) t.i.d. or q.i.d. or 4 inhalations (168 mcg) b.i.d. with dosage reduced based on patient response. Maximum: 10 inhalations (420 mcg) daily. INHALATION AEROSOL (40 MCG,80 MCG [QVAR]) Adults and adolescents.Initial for patients previously taking bronchodilators alone: 1 to 2 inhalations (40 to 80 mcg) b.i.d., depending on strength used. Maximum: 4 to 8 inhalations (320 mcg) b.i.d., depending on strength used. Initial for patients previously taking inhaled corticosteroids: 1 to 4 inhalations (160 mcg) b.i.d., depending on strength used. Maximum: 4 to 8 inhalations (320 mcg) b.i.d., depending on strength used. Children ages 5 to 11. 1 inhalation (40 mcg) b.i.d. Maximum: 1 to 2 inhalations (80 mcg) b.i.d., depending on strength used. To relieve symptoms of seasonal or perennial allergic and nonallergic (vasomotor) rhinitis and prevent nasal polyps from recurring after surgical removal NASAL INHALATION AEROSOL Adults and children age 12 and over. Initial: 1 inhalation (42 mcg) in each nostril b.i.d. to q.i.d. for total dose of 168 to 336 mcg daily. Maintenance: 1 inhalation (42 mcg) in each nostril t.i.d. for total dose of 252 mcg daily. Children ages 6 to 12. 1 inhalation (42 mcg) in each nostril t.i.d. for total dose of 252 mcg daily.
NASAL SPRAY Adults and children age 12 and over. 1 or 2 inhalations (42 or 84 mcg) in each nostril b.i.d. for total dose of 168 or 336 mcg daily.

Mechanism of Action

May decrease number and activity of cells involved in the inflammatory response of asthma, allergies, and rhinitis, such as mast cells, eosinophils, basophils, lymphocytes, macrophages, and neutrophils. Also may inhibit production or secretion of chemical mediators, such as histamine, eicosanoids, leukotrienes, and cytokines. May produce direct smooth-muscle cell relaxation and decrease airway hyperresponsiveness.

Contraindications

Hypersensitivity to beclomethasone’s ingredients, infrequent oral corticosteroid treatment, primary treatment of status asthmaticus or other acute asthma attack, relief of acute bronchospasm or of asthma controlled by bronchodilators or other nonsteroidal , treatment of nonasthmatic bronchitis

Side Efect

CNS: Depression, fatigue, fever, headache, insomnia, light-headedness
CV: Chest pain, tachycardia
EENT: Cataracts, dry mouth, dysphonia, earache, epistaxis, glaucoma, hoarseness, lacrimation, nasal congestion, nose and throat dryness and irritation, oral candidiasis, pharyngitis, rhinorrhea, sinusitis, sneezing, unpleasant smell and taste
ENDO: Adrenal insufficiency, cushingoid symptoms
GI: Diarrhea, indigestion, nausea, rectal hemorrhage
GU: Dysmenorrhea, UTI
MS: Arthralgia, growth suppression in children (nasal aerosol)
RESP: Bronchitis, bronchospasm, chest congestion, cough, pulmonary infiltrates, upper respiratory tract infection, wheezing
SKIN: Acne, eczema, pruritus, rash, skin discoloration, urticaria
Other: Angioedema, flulike symptoms, lymphadenopathy, weight gain

Cautions

If patient also takes an oral corticosteroid, expect to taper dosage slowly (by decreasing daily dosage or taking drug every other day) about 1 week after beclomethasone therapy begins. Expect dosage reductions of more than 2.5 mg daily.
WARNING When gradually switching patient from oral corticosteroid to inhaled beclomethasone, watch for signs of lifethreatening adrenal insufficiency, such as fatigue, lassitude, weakness, nausea, vomiting, and hypotension, during transition period and when exposed to trauma, surgery, infection, or other stressor. If signs occur, notify prescriber immediately.

Expect to resume oral corticosteroid during a stressful period or severe asthma attack.

Because beclomethasone may be absorbed systemically, watch for signs of adrenal insufficiency during periods of stress.

If patient has acute asthma attack or increased wheezing after receiving beclomethasone, give fast-acting bronchodilator, as prescribed. Expect to discontinue beclomethasone.

Assess for signs of candidiasis, such as thick white plaques or coating on tongue and sides of mouth. If present, notify prescriber and expect to reduce dose or frequency or to stop beclomethasone. Also anticipate treatment with antifungal drug.

When administering beclomethasone
NASAL SPRAY, periodically assess nasal discharge for color or consistency changes, which may indicate infection.

Monitor the growth of children receiving beclomethasone nasally.

PATIENT SAFTY

Advise patient not to abruptly stop taking beclomethasone because adrenal insufficiency may occur. Urge her to notify prescriber if she develops signs of adrenal insufficiency, such as nausea, fatigue, anorexia, dyspnea, hypotension, fever, malaise, dizziness, and fainting.

Before patient uses
NASAL SPRAY for first time, instruct her to prime pump by placing her thumb on its base and her index and middle fingers on its shoulder area and then pressing her thumb firmly and quickly against the bottle several times or until fine mist appears. Before patient uses nasal inhalation canister for first time, instruct her to shake it and check that it’s working properly by spraying it once in the air while looking for fine mist.

Teach patient to inhale deeply after each
NASAL SPRAY or inhalation, exhaling through mouth and tilting head back to let drug spread over the nasopharynx.

Teach patient how to properly use oral inhalation aerosol, shaking canister well before using. If patient has trouble using device and coordinating inhalation with it, suggest using a spacer device.

If two inhalations are prescribed, advise patient to wait a minute between them.

If patient uses an inhaled bronchodilator with beclomethasone oral inhalation, tell her to use bronchodilator first, wait 5 minutes, and then use beclomethasone.
WARNING Warn patient that beclomethasone isn’t intended to relieve acute bronchospasm. Urge patient to notify prebeclomethasone dipropionate 130 scriber if asthma symptoms don’t respond.

Advise patient to wear medical identification that states need for supplemental oral corticosteroids during stress or severe asthma attack. Inform patient that prescriber may order high-dose oral corticosteroid therapy.
WARNING Caution patient to avoid exposure to chickenpox and measles because drug may cause immunosuppression. If she’s exposed to these disorders, urge her to notify prescriber immediately.

Category

Chemical class: Tertiary amine
Therapeutic class: GI anticholinergic

Pregnancy category: C

Indications

To treat peptic ulcer disease, functional digestive disorders (including spastic, mucous, and ulcerative colitis), diarrhea, diverticulitis, pancreatitis, dysmenorrhea, nocturnal enuresis, idiopathic and postencephalitic parkinsonism, motion sickness, and nausea and vomiting of pregnancy
Adults. 0.25 to 0.5 mg t.i.d. Children over age 6. 0.125 to 0.25 mg t.i.d. TINCTURE
Adults. 0.6 to 1 ml t.i.d. or q.i.d. Children. 0.03 ml/kg (0.8 ml/m2) t.i.d. Route Onset Peak Duration P.O. 1–2 hr Unknown 4 hr

Mechanism of Action

Inhibits acetylcholine’s muscarinic actions at postganglionic parasympathetic receptor sites, including smooth muscles, secretory glands, and CNS. These actions relax smooth muscles and diminish GI, GU, and biliary tract secretions.

Contraindications

Hepatic disease, hypersensitivity to anticholinergic or scopolamine, ileus, myasthenia gravis, myocardial ischemia, narrowangle glaucoma, obstructive condition of GI or GU tract, renal disease, severe ulcerative colitis, tachycardia, toxic megacolon, unstable cardiovascular status in acute hemorrhage

Interactions

amantadine: Increased adverse anticholinergic effects atenolol, digoxin: Possibly increased therapeutic and adverse effects of these phenothiazines: Possibly decreased phenothiazine effectiveness and increased adverse effects of belladonna alkaloids tricyclic antidepressants: Possibly increased adverse anticholinergic effects

Side Efect

CNS: CNS stimulation (with high doses), confusion, dizziness, drowsiness, headache, insomnia, nervousness, weakness
CV: Bradycardia, palpitations, tachycardia
EENT: Altered taste, blurred vision, dry mouth, increased intraocular pressure, mydriasis, nasal congestion, photophobia
GI: Bloating, constipation, dysphagia, heartburn, ileus, nausea, vomiting
GU: Impotence, urinary hesitancy, urine retention
SKIN: Decreased sweating, flushing, urticaria
Other: Anaphylaxis

Cautions

Avoid using high doses of belladonna alkaloids in ulcerative colitis because they may inhibit intestinal motility and precipitate or aggravate toxic megacolon. Also avoid high doses in hiatal hernia and reflux esophagitis because they may aggravate esophagitis.

Use belladonna alkaloids cautiously in patients with allergies, arrhythmias, asthma, autonomic neuropathy, coronary artery disease, debilitating chronic lung disease, heart failure, hypertension, hyperthyroidism, and prostatic hypertrophy.

Give drug 30 to 60 minutes before a meal.
WARNING Monitor patient for excitement, agitation, drowsiness, and confusion. Elderly patients are more sensitive to the effects of the drug, even small doses, and are more likely to develop adverse reactions. Dosage may need to be decreased.

Take safety precautions to protect patient from injury from falling.

PATIENT SAFTY

Instruct patient to take belladonna alkaloids 30 to 60 minutes before eating.

Tell patient to notify prescriber if she has persistent or severe diarrhea, constipation, or difficulty urinating.

Caution patient to avoid driving and similar activities until the effects of belladonna alkaloids are known.
WARNING Urge patient to avoid extreme heat and humidity because heatstroke could occur.

Category

Chemical class: Ethylester of benazeprilat
Therapeutic class: Antihypertensive

Pregnancy category: D

Indications

To control hypertension alone or with a thiazide diuretic Adults who don’t receive a diuretic.Initial: 10 mg daily. Maintenance: 20 to 40 mg daily as a single dose or in two divided doses. Adults who receive a diuretic. 5 mg daily.
DOSAGE ADJUSTMENT Initial dosage of 5 mg/day for patients with impaired renal function and creatinine clearance less than 30 ml/min/1.73 m2; then increased gradually until blood pressure is controlled or dosage reaches maximum of 40 mg daily. , SUSPENSION Children age 6 and over with glomerular filtration rate of 30 ml/min/1.73 m2or higher. Initial: 0.2 mg/kg daily. Maximum: 0.6 mg/kg daily or 40 mg daily. Route Onset Peak Duration P.O. 1 hr 2–4 hr 24 hr

Mechanism of Action

May reduce blood pressure by affecting renin-angiotensin-aldosterone system. By inhibiting angiotensin-converting enzyme, benazepril:

prevents conversion of angiotensin I to angiotensin II, a potent vasoconstrictor that also stimulates aldosterone release.

may inhibit renal and vascular production of angiotensin II.

decreases serum angiotensin II level and increases serum renin activity. This decreases aldosterone secretion, slightly increasing serum potassium level and fluid loss.

decreases vascular tone and blood pressure.

inhibits aldosterone release, which reduces sodium and water resorption, increases their excretion, and reduces blood pressure.

Contraindications

History of angioedema, hypersensitivity to benazepril or other ACE inhibitor

Interactions

antacids: Possibly decreased bioavailability of benazepril; separate doses by 2 hours antidiabetics (oral): Possibly increased risk of hypoglycemia capsaicin: Possibly induction or exacerbation of ACE cough caused by benazepril digoxin: Increased serum digoxin level diuretics: Possibly excessive hypotension indomethacin: Reduced hypotensive effects of benazepril lithium: Increased serum lithium level and risk of lithium toxicity phenothiazines: Possibly increased therapeutic and adverse effects of benazepril potassium preparations, potassium-sparing diuretics: Possibly increased serum potassium level sodium aurothiomalate: Increased risk of nitritoid reactions, such as facial flushing, nausea, vomiting, and hypotension

Side Efect

CNS: Anxiety, asthenia, dizziness, drowsiness, fatigue, headache, hypertonia, insomnia, nervousness, paresthesia, sleep disturbance, somnolence, syncope, weakness
CV: Angina, ECG changes, hypotension, orthostatic hypotension, palpitations, peripheral edema
EENT: Sinusitis
ENDO: Hyperglycemia
GI: Abdominal pain, constipation, elevated liver function test results, gastritis, melena, nausea, pancreatitis, small bowel angiobenazepril hydrochloride 132 edema, vomiting
GU: Decreased libido, elevated BUN and serum creatinine levels, impotence, nephrotic syndrome, proteinuria, renal insufficiency, UTI
HEME: Agranulocytosis, decreased hemoglobin level, leukopenia, neutropenia, thrombocytopenia
MS: Arthralgia, arthritis, myalgia
RESP: ACE cough, asthma, bronchitis, bronchospasm, dyspnea
SKIN: Dermatitis, diaphoresis, flushing, photosensitivity, pruritus, rash
Other: Anaphylaxis, angioedema, hyperkalemia, hyponatremia

Cautions

Evaluate blood pressure with patient lying down, sitting, and standing before starting benazepril and then every 4 to 8 hours, as appropriate, to monitor effectiveness.

Monitor urine output and BUN and serum creatinine levels, as needed, before therapy.
WARNING Be alert for angioedema, especially after first dose. If it extends to larynx and patient has laryngeal stridor or signs of airway obstruction, prepare to give epinephrine subcutaneously immediately, as prescribed, and discontinue benazepril.

Monitor WBC count periodically to detect neutropenia and agranulocytosis.

Check serum potassium and other electrolyte levels to detect electrolyte imbalances.

To prevent injury caused by orthostatic hypotension, take safety precautions, such as having patient change positions slowly and sit on edge of bed before arising.

PATIENT SAFTY

Teach patient how to monitor blood pressure, if appropriate, and how to recognize signs of hypertension and hypotension.
WARNING Strongly urge patient to contact prescriber before using any OTC salt substitutes, which may contain potassium, or potassium supplements. These substances increase the risk of hyperkalemia.

Explain that a persistent dry cough may develop and may not subside unless benazepril is stopped. If cough becomes bothersome or interferes with sleep or activities, tell her to notify prescriber.
WARNING Instruct patient to contact prescriber immediately if she has signs of angioedema, such as swelling of the face, eyes, lips, or tongue.

Caution patient to avoid sudden position changes and to rise slowly from sitting or lying to minimize orthostatic hypotension.
WARNING Advise patient to stop benazepril and notify prescriber as soon as possible if she experiences syncope.
WARNING Caution women of childbearing age to use reliable contraception and to notify prescriber immediately if pregnancy is suspected. Benazepril may cause fetal harm and should be discontinued.

Category

Chemical class: Para-aminobenzoic acid (tetracaine-like)
Therapeutic class: Nonnarcotic antitussive

Pregnancy category: C

Indications

To relieve cough Adults and children over age 10. 100 mg t.i.d. up to 600 mg daily. Route Onset Peak Duration P.O. 15–20 min Unknown 3–8 hr

Mechanism of Action

Anesthetizes stretch receptors in respiratory tract, lung tissue, and pleura, interfering with their activity and reducing cough reflex at its source. In usual doses, benzonatate doesn’t inhibit respiratory center.

Contraindications

Hypersensitivity to benzonatate or related compounds

Side Efect

CNS: Confusion, hallucinations, headache, mild dizziness, sedation
CV: Cardiogenic shock, chest numbness
EENT: Burning eyes, laryngospasm, nasal congestion
GI: Constipation, GI upset, nausea
RESP: Bronchospasm
SKIN: Pruritus, rash

Cautions

Assess type and frequency of cough. Don’t try to suppress cough with benzonatate if cough has therapeutic benefit, such as to move secretions and improve airflow.
WARNING Don’t break or crush capsules or let patient chew or dissolve them in her mouth. Releasing drug in the mouth may anesthetize mouth and throat, causing risk of choking. Also don’t let patient suck or chew capsule to prevent severe hypersensitivity reaction.

PATIENT SAFTY

Instruct patient to swallow capsules whole and not to chew, suck, or open them.

Warn patient that mild dizziness and sedation may occur. Teach her to take safety measures, and encourage her to avoid activities that require mental alertness until benzonatate’s effects are known.

Category

Chemical class: Benzoquinolizine amide
Therapeutic class: Antiemetic

Pregnancy category: Not rated

Indications

To treat nausea and vomiting related to anesthesia or surgery I.V.OR
I.M.INJECTION
Adults.50 mg or 0.5 to 1 mg/kg I.M., repeated in 1 hr, then every 3 to 4 hr, p.r.n. Or 25 mg or 0.2 to 0.4 mg/kg by slow infusion (1 ml every 0.5 to 1 min) as a single dose. Then, I.M. doses begin. To prevent nausea and vomiting related to anesthesia and surgery
I.M.INJECTION
Adults. 50 mg or 0.5 to 1 mg/kg 15 min before emergence from anesthesia. Route Onset Peak Duration I.V., I.M. 15 min Unknown Unknown

Mechanism of Action

Exhibits antiemetic, antihistaminic, mild cholinergic, and sedative effects by unknown mechanism.

Contraindications

Hypersensitivity to benzquinamide or its components

Interactions

vasopressors: Increased hypertensive effects

Side Efect

CNS: Chills, dizziness, drowsiness, excitement, fatigue, fever, headache, insomnia, nervousness, restlessness, tremor, weakness
CV: Atrial fibrillation, hypertension, hypotension, premature atrial or ventricular contractions
EENT: Blurred vision, dry mouth, increased salivation
GI: Anorexia, hiccups, nausea
MS: Muscle twitching
SKIN: Diaphoresis, flushing, rash, urticaria

Cautions

WARNING Avoid I.V. route in patients with cardiovascular disease because sudden blood pressure increases and transient arrhythmias may occur. Use I.V. route only for patients without cardiovascular disease who aren’t receiving a preanesthetic or cardiovascular drug.

Administer benzquinamide I.M. into large, well-developed muscle. Avoid using deltoid muscle unless it’s well developed.

Take safety precautions to reduce the risk of injury from CNS depression.

PATIENT SAFTY

Advise patient to stay in bed and call for assistance to reduce risk of injury.

Tell patient to report whether nausea and vomiting have been relieved.

Category

Chemical class: Tertiary amine
Therapeutic class: Antiparkinsonian, centralacting anticholinergic

Pregnancy category: C

Indications

As adjunct, to treat all forms of Parkinson’s disease benzquinamide hydrochloride;benztropine mesylate 134 , I.M.OR
I.V.INJECTION Adults with Parkinson’s disease.1 to 2 mg daily (usual dose) with a range of 0.5 to 6 mg daily. Adults with idiopathic Parkinson’s disease.Initial: 0.5 to 1 mg at bedtime. Maximum: 4 to 6 mg daily. Adults with postencephalitic Parkinson’s disease. 2 mg daily in one or more doses; may begin with 0.5 mg at bedtime and increase as needed. To control extrapyramidal symptoms (except tardive dyskinesia) caused by phenothiazines and other neuroleptics , I.M.OR
I.V.INJECTION
Adults. 1 to 4 mg once or twice daily. To treat acute dystonic reactions , I.M.OR
I.V.INJECTION
Adults. Initial: 1 to 2 ml (1 to 2 mg total dose) I.V. or I.M. Maintenance: 1 to 2 mg P.O. b.i.d. to prevent recurrence. Route Onset Peak Duration P.O. 1–2 hr Unknown 24 hr I.V., I.M 15 min Unknown 24 hr

Mechanism of Action

Blocks acetylcholine’s action at cholinergic receptor sites. This restores the brain’s normal dopamine and acetylcholine balance, which relaxes muscle movement and decreases drooling, rigidity, and tremor. Benztropine also may inhibit dopamine reuptake and storage, which prolongs dopamine’s action.

Contraindications

Achalasia, bladder neck obstruction, glaucoma, hypersensitivity to benztropine mesylate or its components, megacolon, myasthenia gravis, prostatic hypertrophy, pyloric or duodenal obstruction, stenosing peptic ulcer

Interactions

amantadine: Possibly increased adverse anticholinergic effects digoxin: Possibly increased digoxin level
haloperidol: Possibly increased schizophrenic symptoms, decreased serum haloperidol level, and development of tardive dyskinesia levodopa: Possibly decreased levodopa effectiveness phenothiazines: Possibly reduced phenothiazine effects and increased psychiatric symptoms

Side Efect

CNS: Agitation, confusion, delirium, delusions, depression, disorientation, dizziness, drowsiness, euphoria, excitement, fever, hallucinations, headache, light-headedness, listlessness, memory loss, nervousness, paranoia, psychosis, weakness
CV: Hypotension, mild bradycardia, orthostatic hypotension, palpitations, tachycardia
EENT: Blurred vision, diplopia, dry mouth, increased intraocular pressure, mydriasis, narrow-angle glaucoma, suppurative parotitis
GI: Constipation, duodenal ulcer, epigastric distress, ileus, nausea, vomiting
GU: Dysuria, urinary hesitancy, urine retention
MS: Muscle spasms, muscle weakness
SKIN: Decreased sweating, dermatoses, flushing, rash, urticaria

Cautions

Expect to administer I.V. or I.M. benztropine when patient needs more rapid response than oral drug can provide. Be aware that I.M. route is commonly used because it provides effects in about the same time as I.V. route. Watch for improvement a few minutes after administration. If Parkinsonian symptoms reappear, expect to repeat dose.

Therapy typically begins with a low dose followed by gradual increases of 0.5 mg every 5 or 6 days because benztropine has a cumulative action.

Assess muscle rigidity and tremor at baseline. Then monitor them often for improvement, which indicates drug’s effectiveness.

Give drug before or after meals based on patient’s need and response. If patient has increased salivary secretions, expect to administer benztropine after meals. If patient has dry mouth, plan to give drug before meals unless nausea develops.
WARNING When giving drug to patient with drug-induced extrapyramidal reactions, watch for worsening psychiatric symptoms.

High-dose benztropine therapy may cause weakness and inability to move specific muscle groups. If this occurs, expect to reduce benztropine dosage.

PATIENT SAFTY

Warn patient that drug has a cumulative effect, increasing risk of

Side Efect

and overdose.

Caution against driving and similar activities until benztropine’s effects are known because it may cause blurred vision, dizziness, or drowsiness.
WARNING Because benztropine decreases sweating, urge patient to avoid extremely hot or humid conditions to reduce risk of heatstroke and severe hyperthermia. This is especially important for elderly patients and those who abuse alcohol or have chronic illness or CNS disease.

Stress need for periodic eye examinations and intraocular pressure measurements because drug may cause narrow-angle glaucoma and increase intraocular pressure.

Category

Chemical class: Calcium channel blocker, diarylammopropylamine derivative
Therapeutic class: Antianginal

Pregnancy category: C

Indications

To treat chronic stable angina in patients who don’t respond to or can’t tolerate other antianginal
Adults. Initial: 200 mg daily for 10 days followed by dosage increases, depending on patient’s response (ability to perform daily activities, length of QT interval, heart rate, and frequency and severity of angina attacks). Maintenance: 300 to 400 mg daily (maximum). Route Onset Peak Duration P.O. Unknown 8 days Unknown

Mechanism of Action

Inhibits calcium movement into coronary and vascular smooth-muscle cells by blocking slow calcium channels in their membranes. This decreases intracellular calcium level, which inhibits smooth-muscle cell contractions and causes:

relaxation of coronary and vascular smooth muscles, decreased peripheral vascular resistance, and reduced systolic and diastolic blood pressure, which decrease myocardial oxygen demand

depression of impulse formation (automaticity) and conduction velocity. Bepridil also inhibits fast inward sodium channels, reducing speed and degree of action potential and increasing its duration in cardiac muscle.

Contraindications

Congenital prolonged QT interval, history of serious ventricular arrhythmias, hypersensitivity to bepridil, hypotension (systolic pressure below 90 mm Hg), sick sinus syndrome and secondor third-degree AV block unless artificial pacemaker in place, uncompensated cardiac insufficiency, use of other that prolong QT interval

Interactions

antiarrhythmics, such as quinidine and procainamide, with actions similar to bepridil’s: Exaggerated and prolonged QT interval
beta blockers: Possibly increased depression of myocardial contractility and AV conduction digoxin: Possibly increased serum digoxin level fentanyl: Severe hypotension and increased need for fluid nitrates: Additive hypotensive effect tricyclic antidepressants: Exaggerated and prolonged QT interval

Side Efect

CNS: Amnesia, anxiety, asthenia, depression, dizziness, drowsiness, fever, hallucinations, headache, insomnia, nervousness, paranoia, paresthesia, psychosis, syncope, tremor, vertigo
CV: Edema, hypertension, palpitations, premature ventricular contractions, prolonged QT interval, sinus bradycardia or tachycardia, torsades de pointes, vasodilation, ventricular fibrillation, ventricular tachycardia
EENT: Altered taste, blurred vision, dry mouth, pharyngitis, rhinitis, tinnitus
GI: Abdominal cramps or discomfort, anorexia, appetite increase, constipation, diarbepridil hydrochloride 136 rhea, flatulence, gastritis, nausea
GU: Decreased libido, impotence
HEME: Agranulocytosis, leukopenia, neutropenia
MS: Arthritis, myalgia
RESP: Cough, dyspnea, respiratory tract infection
SKIN: Dermatitis, diaphoresis, rash
Other: Flulike symptoms

Cautions

Use bepridil cautiously in patients with heart failure because it can induce new arrhythmias and may worsen heart failure.

Because bepridil is metabolized by the liver and its metabolites are excreted in urine, monitor results of liver function studies as well as BUN and serum electrolyte and creatinine levels as appropriate.

Assess patient’s heart rate and rhythm to obtain baseline. Then monitor frequently during therapy. Also, monitor serial 12lead ECG tracings. Be aware that bepridil can induce new arrhythmias, including ventricular tachycardia and fibrillation (which are more difficult to convert), torsades de pointes, and prolonged QT intervals.
WARNING Be alert for QT intervals that exceed 0.52 second. If this occurs, expect to reduce bepridil dose or discontinue drug.

Monitor WBC count to detect agranulocytosis, which may warrant stopping bepridil therapy.
WARNING Be aware that bepridil shouldn’t be discontinued abruptly. Instead, gradually taper dosage as prescribed to prevent increased frequency and duration of chest pain as increased calcium moves into cells, causing coronary artery spasm.

Monitor blood pressure often if patient takes a nitrate or beta blocker. Assess for hypotension.

Monitor serum electrolyte levels. Especially note decreased potassium level, which may worsen existing arrhythmias or induce new ones.

PATIENT SAFTY

Advise patient to avoid driving and other activities that require alertness and coordination until bepridil’s CNS effects are known.

Category

Chemical class: Synthetic glucocorticoid
Therapeutic class: Anti-inflammatory

Pregnancy category: C

Indications

To treat conditions with severe inflammation and conditions requiring immunosuppression SYRUP,(BETAMETHASONE)
Adults. 0.6 to 7.2 mg daily.
I.M.INJECTION(BETAMETHASONE ACETATEBETAMETHASONE SODIUM PHOSPHATE)
Adults. 0.5 to 9 mg I.M. daily, or one-third to one-half of P.O. dose every 12 hr. I.M.OR
I.V.INJECTION(BETAMETHASONE SODIUM PHOSPHATE)
Adults.Initial: Variable (given in emergency situations or when oral therapy isn’t possible). Maximum: 9 mg daily. To treat bursitis, gouty arthritis, osteoarthritis, periostitis of cuboid, peritendinitis, rheumatoid arthritis, skin lesions, tenosynovitis INTRA-ARTICULAR,INTRABURSAL,ORINTRADERMAL INJECTION(BETAMETHASONEACETATEBETAMETHASONESODIUMPHOSPHATE) Adults with bursitis,peritendinitis,or tenosynovitis.1 ml by intrabursal or intraarticular injection. Three or four injections given every 1 to 2 wk. Adults with osteoarthritis or rheumatoid arthritis. 0.5 to 2 ml, based on joint size. Adults with foot bursitis.0.25 to 0.5 ml every 3 to 7 days. betamethasone 137 B Adults with foot tenosynovitis or periostitis of cuboid. 0.5 ml every 3 to 7 days. Adults with acute gouty arthritis. 0.5 to 1 ml every 3 to 7 days. Adults with skin lesions. 0.2 ml/cm2intradermally, up to 1 ml weekly.
DOSAGE ADJUSTMENT Dosage reduced for elderly patients and accompanied by periodic monitoring of blood pressure and blood glucose and electrolyte levels. Route Onset Peak Duration P.O. Unknown 1–2 hr 3.25 days I.V., I.M.*Rapid Unknown Unknown I.M. 1–3 hr Unknown 1 wk Other Unknown Unknown 1–2 wk

Mechanism of Action

Binds to intracellular glucocorticoid receptors and suppresses inflammatory and immune responses by:

inhibiting neutrophil and monocyte accumulation at inflammation site and suppressing their phagocytic and bactericidal activity

stabilizing lysosomal membranes

suppressing antigen response of macrophages and helper T cells

inhibiting synthesis of inflammatory response mediators, such as cytokines, interleukins, and prostaglandins.

Contraindications

Idiopathic thrombocytopenic purpura (I.M. injection), live virus vaccination, systemic fungal infection

Interactions

anticholinesterase : Possibly antagonized anticholinesterase effects in myasthenia gravis barbiturates: Possibly decreased effects of betamethasone cyclosporine: Possibly increased risk of cyclosporine toxicity digitalis glycosides: Possibly increased risk of digitalis toxicity estrogens: Possibly decreased excretion of betamethasone hydantoins,
rifampin: Possibly increased excretion and decreased therapeutic effects of betamethasone isoniazid: Possibly decreased serum isoniazid level
ketoconazole: Possibly decreased excretion of betamethasone oral anticoagulants: Possibly increased or decreased action of anticoagulants, requiring adjusted anticoagulant dosage oral contraceptives: Possibly increased halflife and concentration and decreased excretion of betamethasone potassium-wasting diuretics: Increased risk of hypokalemia salicylates: Possibly decreased serum level and therapeutic effects of salicylates somatrem: Possibly inhibition of somatrem’s growth-promoting effects theophyllines: Possibly changes in both ’ effects

Side Efect

CNS: Fatigue, headache, increased intracranial pressure with papilledema, insomnia, malaise, neuritis, paresthesia, seizures, steroid psychosis, syncope, vertigo
CV: Arrhythmias, ECG changes, fat embolism, heart failure, hypertension, thromboembolism, thrombophlebitis
EENT: Cataracts, exophthalmos, glaucoma, increased intraocular pressure
ENDO: Cushingoid symptoms (buffalo hump, central obesity, decreased carbohydrate tolerance, fat pad enlargement, moon face), fluid retention, growth suppression in children, hyperglycemia, masked signs of infection, negative nitrogen balance, secondary adrenocortical and pituitary unresponsiveness (in times of stress)
GI: Abdominal distention, increased appetite, nausea, pancreatitis, peptic ulcer possibly with perforation, ulcerative esophagitis, vomiting
GU: Amenorrhea, glycosuria, menstrual irregularities
HEME: Leukocytosis
MS: Aseptic necrosis of femoral and humeral heads, loss of muscle mass, muscle weakness, osteoporosis, spontaneous pathologic and vertebral compression fractures, tendon rupture betamethasone 138 * Sodium phosphate. Acetate-sodium phosphate. For intra-arterial or intrasynovial injection; 1 week for intralesional injection in soft tissue.
SKIN: Acneiform lesions, allergic dermatitis, ecchymosis, facial erythema, hirsutism, impaired wound healing, increased sweating, petechiae, lupuslike lesions, purpura, subcutaneous fat atrophy, thin and fragile skin, urticaria
Other: Angioedema, hypocalcemia, hypokalemia, sodium retention, suppressed reaction to skin tests, weight gain

Cautions

Expect prescriber to order baseline ophthalmologic examination before starting therapy because prolonged betamethasone use may lead to increased intraocular pressure, glaucoma, and optic nerve damage. Use betamethasone cautiously in patients with ocular herpes simplex because corneal perforation may occur.

Determine if latent or active amebiasis has been ruled out in patients who have spent time in the tropics or who have unexplained diarrhea before betamethasone therapy starts because drug may worsen it.
WARNING Give betamethasone with extreme care in patients with known or suspected Strongyloides (threadworm) infestation because corticosteroids such as betamethasone may result in immunosuppression, Strongyloides hyperinfection and dissemination, and widespread larval migration, resulting in severe enterocolitis and potentially life-threatening gram-negative septicemia.

Assess for signs of infection before administering betamethasone because drug may mask those signs. Because drug may cause immunosuppression, new infection may develop during therapy. If so, expect to administer appropriate antibiotic.

Review serum electrolyte levels, as ordered, before starting therapy. Monitor these levels often during therapy to detect imbalances. Sodium and water retention and potassium and calcium depletion may occur with high-dose betamethasone therapy. If so, expect to restrict sodium intake and provide potassium and calcium supplements.

Because betamethasone is linked to peptic ulcer formation, expect to administer it with an antacid or H2-receptor blocker.
WARNING Monitor ECG tracings for arrhythmias, and evaluate patient for anaphylactic reactions, such as angioedema and seizures, which have been associated with rapid I.V. administration of highdose corticosteroids.
WARNING During long-term betamethasone therapy, assess for signs of adrenal suppression and insufficiency (fatigue, hypotension, lassitude, nausea, vomiting, and weakness) when patient is exposed to stress. If she exhibits these signs, notify prescriber at once.

Watch for signs of steroid psychosis, such as delirium, clouded sensorium, euphoria, insomnia, mood swings, personality changes, and severe depression, which may develop 15 to 30 days after therapy begins. Expect to stop therapy. If this isn’t possible, expect to give psychotropic .

Rotate I.M. injection sites. To prevent muscle atrophy, avoid subcutaneous injection, injection in deltoid site, and repeated I.M. injections into same site.

Administer oral betamethasone before 9 a.m., if appropriate, to mimic body’s natural release of corticosteroids.

After intra-articular injection, assess joint for marked increase in pain, local swelling, and more restricted movement. If patient also develops fever and malaise, suspect septic arthritis and notify prescriber immediately. Expect to assist with joint fluid aspiration to confirm septic arthritis.

Monitor patient for cushingoid signs and symptoms, such as moon face, buffalo hump, central obesity, striae, acne, ecchymosis, and weight gain. Notify prescriber if you detect these symptoms.

Expect to slowly taper oral betamethasone dosage to prevent adrenal insufficiency.

PATIENT SAFTY

Instruct patient to take betamethasone with food if GI upset occurs.

Review signs of adrenal insufficiency and possible need for dosage increases during stress. Advise patient to notify prescriber immediately if signs of insufficiency occur or if she’s exposed to stress.

Instruct patient to avoid exposure to infections because drug can cause immunosuppression. Also teach patient to recognize and immediately report signs of infection.

After intra-articular use, advise patient not to overuse joint and to continue other treatments such as physical therapy. betamethasone

Category

Chemical class: Selective beta1-adrenergic blocker
Therapeutic class: Antihypertensive

Pregnancy category: C

Indications

To treat hypertension alone or with other antihypertensives
Adults. Initial: 10 mg daily. If no response in 7 to 14 days, then 20 mg daily.
DOSAGE ADJUSTMENT For elderly patients and patients who have renal failure or are undergoing hemodialysis, initial dosage reduced to 5 mg daily. If desired response isn’t achieved, dosage increased by 5-mg increments every 2 wk up to 20 mg daily. Route Onset Peak Duration P.O. Unknown 3–4 hr Unknown

Mechanism of Action

Inhibits stimulation of beta1-adrenergic receptor sites, primarily in the heart. This decreases myocardial excitability, cardiac output, and myocardial oxygen demand. It also decreases renin release from the kidneys, which helps reduce blood pressure.

Contraindications

Cardiogenic shock, heart failure unless caused by tachyarrhythmia or overt heart failure, hypersensitivity to betaxolol, secondor third-degree heart block, sinus bradycardia

Interactions

aluminum salts, barbiturates, calcium salts, cholestyramine, colestipol, NSAIDs, penicillins, rifampin, salicylates, sulfinpyrazone: Decreased therapeutic and adverse effects of betaxolol amiodarone, beta blockers, digoxin: Increased risk of additive systemic beta blockade, especially bradycardia calcium channel blockers: Possibly increased therapeutic and adverse effects of betaxolol ciprofloxacin, other quinolones: Possibly increased bioavailability of betaxolol, increasing the drug’s pharmacologic effect
clonidine: Possibly severe hypertension when both (or just clonidine) are simultaneously withdrawn disopyramide: Possibly severe bradycardia, asystole, and heart failure epinephrine: Possibly severe hypertension followed by bradycardia ergot alkaloids: Possibly peripheral ischemia and gangrene flecainide: Possibly increased therapeutic and adverse effects of both lidocaine: Possibly increased risk of lidocaine toxicity nondepolarizing neuromuscular blockers: Possibly increased or decreased neuromuscular blockade oral contraceptives: Possibly increased bioavailability and plasma level of betaxolol, increasing pharmacologic effect prazosin: Possibly increased orthostatic hypotension
quinidine: Possibly increased effects of betaxolol sulfonylureas: Possibly masking of hypoglycemic symptoms

Side Efect

CNS: Amnesia, anxiety, behavior changes, confusion, depression, dizziness, emotional lability, fatigue, fever, hallucinations, headache, insomnia, lethargy, malaise, mood changes, nightmares, paresthesia, peripheral neuropathy, sedation, stroke, syncope, tremor, vertigo
CV: Arrhythmias, including asystole, bradycardia, heart block, and torsades de pointes; cardiogenic shock; chest pain; claudication; heart failure; hypercholesterolemia; hyperlipidemia; hypotension; mitral insufficiency; MI; orthostatic hypotension; peripheral vascular insufficiency; Raynaud’s phenomenon; renal and mesenteric artery thrombosis
EENT: Altered taste, blurred vision, burning eyes, conjunctivitis, dry eyes, dry mouth, earache, eye irritation, eye pain or pressure, increased salivation, laryngospasm, mouth ulcers, nasal stuffiness, pharyngitis, ptosis, rhinitis, sinusitis, tinnitus
ENDO: Breast pain (women), hyperglycemia, hypoglycemia
GI: Acute pancreatitis, anorexia, bloating, constipation, diarrhea, elevated liver funcbetaxolol hydrochloride 140 tion test results, epigastric pain, flatulence, gastritis, heartburn, hepatomegaly, increased appetite, indigestion, nausea, vomiting
GU: Decreased libido, dysuria, impotence, nocturia, Peyronie’s disease, prostatitis, renal colic, renal failure, urinary frequency, urine retention, UTI
HEME: Agranulocytosis, eosinophilia, leukopenia, thrombocytopenia
MS: Arthralgia, arthritis, gout, muscle spasms or twitching, myalgia, neck pain, tendinitis
RESP: Bronchial obstruction, bronchitis, bronchospasm, cough, pulmonary embolus, respiratory distress, upper respiratory tract infection, wheezing
SKIN: Acne, aggravation of psoriasis, diaphoresis, dry skin, eczema, erythema, exfoliative dermatitis, flushing, increased pigmentation, pallor, photophobia, pruritus, rash
Other: Acidosis, facial edema, hyperkalemia, hyperuricemia, lupus erythematosus, lymphadenopathy, positive ANA titer, weight gain

Cautions

Betaxolol shouldn’t be given to patients with untreated pheochromocytoma.

Use drug cautiously in peripheral vascular disease. Assess color, temperature, and pulses in arms and legs, and ask about numbness, tingling and pain.

Check blood pressure with patient lying, sitting, and standing before starting betaxolol therapy and periodically throughout the day to detect changes.

Review renal function test results before and during therapy.

Closely monitor diabetic patient for hypoglycemia because betaxolol may mask tachycardia, but not dizziness and diaphoresis. Be aware that betaxolol may mask tachycardia and blood pressure changes associated with hyperthyroidism.
WARNING Avoid abrupt withdrawal of betaxolol, which can worsen or cause thyroid storm. Expect to withdraw drug gradually and monitor patient closely.

Expect to taper betaxolol over 2 weeks to prevent MI, ventricular arrhythmias, and possibly death from catecholamine hypersensitivity caused by beta blocker therapy.

If systolic pressure falls below 90 mm Hg, expect to discontinue drug and prepare for hemodynamic monitoring.

Take precautions to prevent injury from falls caused by orthostatic hypotension.

PATIENT SAFTY

Teach patient how to check her blood pressure, if appropriate. Also discuss signs and symptoms of hypertension and hypotension.

Advise patient to avoid sudden position changes and to rise slowly from a sitting or lying position to minimize the effects of orthostatic hypotension.

Advise patient to avoid driving and activities that require mental alertness until drug’s CNS effects are known.

Counsel patient to consult prescriber before using an OTC product, such as a cold remedy or nasal decongestant.

Category

Chemical class: Synthetic choline ester
Therapeutic class: Cholinergic, parasympathomimetic

Pregnancy category: C

Indications

To treat postoperative and postpartal urine retention and retention caused by neurogenic atony of bladder
Adults. 10 to 50 mg t.i.d. or q.i.d. To determine minimum effective dose: 5 to 10 mg repeated every hr until response is obtained or maximum of 50 mg is reached. SUBCUTANEOUS INJECTION
Adults. 2.5 to 5 mg t.i.d. or q.i.d. To determine minimum effective dose: 2.5 mg repeated every 15 to 30 min until response is obtained or maximum of four doses is reached. Minimum effective dose may be repeated t.i.d. or q.i.d., p.r.n.

Mechanism of Action

Acts directly on muscarinic receptors of the parasympathetic nervous system, increasing detrusor muscle tone in the bladder and allowing contraction strong enough to start voiding. Like natural neurotransmitter acetylcholine, bethanechol stimulates gastric motility, increases gastric tone, and enhances peristalsis. Route Onset Peak Duration P.O. 30–90 min 60 min 6 hr SubQ 5–15 min 15–30 min 2 hr

Contraindications

Acute inflammatory lesions of GI tract, atrioventricular conduction defects, bronchial asthma, coronary artery disease, epilepsy, hypersensitivity to bethanecol or its components, hypertension, hyperthyroidism, hypotension, marked vagotonia, mechanical obstruction of GI or GU tract, Parkinson’s disease, peptic ulcer disease, peritonitis, pronounced bradycardia, questionable integrity of GI or GU mucosa, spastic GI disorders, vasomotor instability

Interactions

cholinergic : Possibly increased effects of bethanechol ganglionic blockers: Possibly severe hypotension, usually first manifested by severe adverse GI reactions procainamide,
quinidine: Possibly decreased effects of bethanechol

Side Efect

CNS: Headache, malaise
CV: Hypotension with reflex tachycardia, vasomotor response
EENT: Excessive salivation, lacrimation, miosis
GI: Abdominal cramps, colicky pain, diarrhea, eructation, nausea, vomiting
GU: Urinary urgency
RESP: Asthma attack, bronchoconstriction

Cautions

Assess urine elimination before starting bethanechol therapy.
WARNING Be aware that patient must have functioning urinary sphincter because a sphincter that doesn’t relax when bladder contracts can push urine upward into renal pelvis and cause reflux infection.

Give oral bethanechol 1 hour before or 2 hours after meals to reduce risk of nausea and vomiting.
WARNING Don’t give bethanechol I.M. or I.V. because of risk of cholinergic overstimulation, which can cause abdominal cramps, bloody diarrhea, hypotension, shock, or sudden cardiac arrest. Always keep atropine nearby during subcutaneous administration.

PATIENT SAFTY

Advise patient to take bethanechol on an empty stomach 1 hour before or 2 hours after meals to reduce risk of nausea and vomiting.

Category

Chemical class: Tertiary amine
Therapeutic class: Anticholinergic, antidyskinetic

Pregnancy category: C

Indications

As adjunct to treat all forms of Parkinson’s disease
Adults. 2 mg t.i.d. or q.i.d up to 16 mg daily. To control extrapyramidal symptoms (except tardive dyskinesia) caused by phenothiazines and other neuroleptic
Adults. 2 mg one to three times daily. I.V.OR
I.M.INJECTION
Adults. 2 mg repeated every 30 min until symptoms resolve or maximum of four consecutive doses in 24 hr is reached. Route Onset Peak Duration I.V. 15 min Unknown 1–8 hr I.M. 10–30 min Unknown Unknown

Mechanism of Action

Blocks acetylcholine’s action at cholinergic receptor sites. This action restores the brain’s normal dopamine and acetylcholine biperiden 142 balance, which relaxes muscle movement and decreases rigidity and tremors. Biperiden also may inhibit dopamine reuptake and storage, which prolongs dopamine’s action.

Contraindications

Achalasia, bladder neck obstruction, hypersensitivity to biperiden, myasthenia gravis, narrow-angle glaucoma, prostatic hypertrophy, pyloric or duodenal obstruction, stenosing peptic ulcer, toxic megacolon

Interactions

amantadine: Possibly increased adverse anticholinergic effects digoxin: Possibly increased serum digoxin level
haloperidol: Possibly increased schizophrenic symptoms, decreased serum haloperidol level, and development of tardive dyskinesia levodopa: Possibly decreased levodopa effectiveness phenothiazines: Possibly reduced phenothiazine effects and increased psychiatric symptoms

Side Efect

CNS: Agitation, confusion, delirium, delusions, depression, disorientation, dizziness, drowsiness, euphoria, excitement, fever, hallucinations, headache, light-headedness, listlessness, memory loss, nervousness, paranoia, psychosis, weakness
CV: Hypotension, mild bradycardia, orthostatic hypotension, palpitations, tachycardia
EENT: Blurred vision, diplopia, dry mouth, increased intraocular pressure, mydriasis, narrow-angle glaucoma, suppurative parotitis
GI: Constipation, duodenal ulcer, epigastric distress, ileus, nausea, vomiting
GU: Dysuria, urinary hesitancy, urine retention
MS: Muscle spasms, muscle weakness
SKIN: Decreased sweating, dermatosis, flushing, rash, urticaria

Cautions

Expect to give I.V. or I.M. biperiden when patient needs more rapid response than oral drug can provide.

Assess muscle rigidity and tremor as baseline. Then check them often for improvement, indicating biperiden’s effectiveness.
WARNING When giving biperiden to patient with drug-induced extrapyramidal reactions, be alert for worsening of psychiatric symptoms.

PATIENT SAFTY

Caution patient to avoid driving and other activities that require alertness until biperiden’s CNS effects are known.
WARNING Because biperiden decreases sweating, urge patient to avoid extremely hot and humid conditions to reduce risk of heatstroke and severe hyperthermia. This is especially important for elderly patients and those who abuse alcohol or have chronic illness or CNS disease.

Emphasize the need for periodic eye examinations and intraocular pressure measurement because biperiden may cause narrow-angle glaucoma and increase intraocular pressure.

Category

Chemical class: Selective beta1-adrenergic blocker
Therapeutic class: Antihypertensive

Pregnancy category: C

Indications

To treat hypertension, alone or with other antihypertensives
Adults. 5 mg daily, increased to 10 to 20 mg daily if blood pressure doesn’t respond to lower dosage.
DOSAGE ADJUSTMENT Dosage reduced to 2.5 mg daily initially and then increased gradually for patients with impaired renal function and creatinine clearance less than 40 ml/min/1.73 m2or who have impaired hepatic function, as from cirrhosis or hepatitis.

Mechanism of Action

Inhibits stimulation of beta1-receptors primarily in the heart, which decreases cardiac excitability, cardiac output, and myocardial oxygen demand. Bisoprolol also decreases renin release from kidneys, which helps reduce blood pressure.

Contraindications

Cardiogenic shock, heart failure unless caused by tachyarrhythmia, overt heart failure, secondor third-degree heart block, sinus bradycardia

Interactions

aluminum salts, barbiturates, calcium salts, cholestyramine, colestipol, NSAIDs, penicillins, rifampin, salicylates, sulfinpyrazone: Possibly decreased therapeutic and adverse effects of bisoprolol beta blockers, digoxin: Increased risk of bradycardia calcium channel blockers: Possibly increased therapeutic and adverse effects of bisoprolol ciprofloxacin, quinolones: Possibly increased bioavailability of bisoprolol
clonidine: Possibly severe hypertension from withdrawal of clonidine or both epinephrine: Possibly hypertension followed by bradycardia ergot alkaloids: Possibly peripheral ischemia and gangrene flecainide: Possibly increased therapeutic and adverse effects of either drug lidocaine: Possibly increased risk of lidocaine toxicity oral contraceptives: Possibly increased bioavailability and plasma level of bisoprolol prazosin: Possibly increased orthostatic hypotension
quinidine: Possibly increased bisoprolol effects sulfonylureas: Possibly masking of hypoglycemic symptoms

Side Efect

CNS: Anxiety, confusion, depression, dizziness, emotional lability, fatigue, fever, hallucinations, headache, insomnia, malaise, nightmares, paresthesia, sleep disturbances, syncope, tremor, unsteadiness, vertigo
CV: Bradycardia, heart block, and other arrhythmias; chest pain; claudication; cold arms and legs; edema; heart failure; hypercholesterolemia; hyperlipidemia; hypotension; MI; orthostatic hypotension; palpitations; peripheral vascular insufficiency; renal and mesenteric artery thrombosis
EENT: Altered taste, blurred vision, dry mouth, eye pain or pressure, hearing loss, increased salivation, laryngospasm, pharyngitis, rhinitis, sinusitis, tinnitus
GI: Constipation, diarrhea, epigastric pain, gastritis, indigestion, ischemic colitis, nausea, vomiting
GU: Cystitis, decreased libido, impotence, Peyronie’s disease, renal colic
HEME: Agranulocytosis, eosinophilia, leukopenia, thrombocytopenia, thrombocytopenic purpura
MS: Arthralgia, gout, muscle twitching, neck pain
RESP: Asthma, bronchitis, bronchospasm, cough, dyspnea, respiratory distress, upper respiratory tract infection
SKIN: Alopecia, dermatitis, diaphoresis, eczema, exfoliative dermatitis, flushing, pruritus, psoriasis, rash
Other: Angioedema, hyperkalemia, hyperuricemia, weight gain

Cautions

Administer bisoprolol cautiously in patients with peripheral vascular disease because reduced cardiac output can cause or worsen arterial insufficiency. Assess patient’s arms and legs for changes in color, temperature, and pulses; ask about numbness, tingling, and pain.

Measure blood pressure with patient lying, sitting, and standing before starting bisoprolol and then every 4 to 8 hours, as appropriate, to evaluate effectiveness.

If patient has diabetes, monitor closely for signs of hypoglycemia, which drug may mask.

If patient has hyperthyroidism, watch for tachycardia and hypertension, which may be masked by bisoprolol.
WARNING Keep in mind that abrupt withdrawal of bisoprolol may cause or worsen thyroid storm. During drug withdrawal, monitor patient closely.

Expect to stop bisoprolol over 1 to 2 weeks to prevent MI, ventricular arrhythmias, and, possibly, death from catecholamine hypersensitivity caused by beta blocker therapy.

If systolic blood pressure falls to less than 90 mm Hg, expect to discontinue drug. Prepare for hemodynamic monitoring, if needed.
WARNING If patient is scheduled for surgery with general anesthesia, expect to discontinue bisoprolol about 48 hours beforehand to reduce risk of excessive myocardial depression during anesthesia. bisoprolol fumarate 144

PATIENT SAFTY

Teach patient how to monitor her blood pressure, if appropriate, and to recognize signs of hypertension and hypotension.

Instruct patient to avoid sudden position changes and to rise slowly from a sitting or lying position to minimize the effects of orthostatic hypotension.

Advise patient to avoid driving and other activities that require mental alertness until bisoprolol’s CNS effects are known.

Instruct patient to contact prescriber before using any OTC product, such as a cold remedy or nasal decongestant.

Category

Chemical class: Acid ester of colterol
Therapeutic class: Bronchodilator, sympathomimetic

Pregnancy category: C

Indications

To prevent and treat asthma and other conditions associated with reversible bronchospasm, such as emphysema and chronic bronchitis INTERMITTENT AEROSOL SOLUTION Adults and children age 12 and over. 1 mg bitolterol diluted in 0.5 ml normal saline solution and inhaled over 10 to 15 min t.i.d. Maximum: 8 mg daily. CONTINUOUS AEROSOL SOLUTION Adults and children age 12 and over. 2.5 mg bitolterol diluted in 1.25 ml normal saline solution and inhaled over 10 to 15 min t.i.d. Maximum: 14 mg daily. METERED-DOSE INHALER Adults and children age 12 and over. To treat acute bronchospasm: 2 inhalations over 1 to 3 min and, if needed, a third inhalation. To prevent bronchospasm: 2 inhalations every 8 hr, not to exceed 3 inhalations every 6 hr or 2 inhalations every 4 hr.

Mechanism of Action

Is hydrolyzed to active agent colterol (a long-acting agent that primarily affects beta2-adrenergic receptors). Then it attaches to beta2receptors on bronchial cell membranes. This action stimulates the intracellular enzyme adenylate cyclase to convert adenosine triphosphate to cyclic adenosine monophosphate (cAMP). An increased intracellular level of cAMP relaxes bronchial smooth-muscle cells, stabilizes mast cells, and inhibits histamine release. Route Onset Peak Duration Aerosol, 2–3 min 30–60 min 6–8 hr inhalation Metered3–5 min 30–120 min 4–8 hr dose inhalation

Incompatibilities

Don’t mix bitolterol in inhalation solution with cromolyn sodium or acetylcysteine.

Contraindications

Hypersensitivity to bitolterol or ingredients

Interactions

beta blockers: Possibly inhibition of bronchodilating effect of bitolterol epinephrine, other sympathomimetic : Possibly additive effects of either drug MAO inhibitors, tricyclic antidepressants: Possibly potentiation of bitolterol’s action on cardiovascular system

Side Efect

CNS: Dizziness, fatigue, headache, hyperkinesia, insomnia, light-headedness, nervousness, paresthesia, somnolence, tremor, vertigo
CV: Chest pain, hypertension, irregular pulse, palpitations, tachycardia, transient ECG changes
EENT: Mouth and throat irritation, rhinitis
GI: Elevated liver function test results, nausea
HEME: Decreased hemoglobin level, hematocrit, and WBC count
RESP: Bronchospasm, cough

Cautions

Assess respiratory rate, rhythm, and depth and breath sounds before, during, and after bitolterol therapy. Expect improved air movement and improvement in abnormal breath sounds.

Because beta-adrenergic bronchodilators can significantly increase blood pressure and pulse rate, monitor them often.

Expect therapy to begin with lowest effective dose because higher doses or more frequent use may reduce effectiveness and cause paradoxical reactions or overdose.

PATIENT SAFTY

Teach patient how to properly use and care for aerosol nebulizer or metered-dose inhaler. Before patient uses aerosol nebulizer, advise her to look for slight bubbling in solution-filled chamber and fine mist when nebulizer is turned on. Before patient uses inhaler for first time, instruct her to make sure it’s working properly by spraying it once in the air and looking for fine mist.

Teach patient to mix nebulizer solution immediately before use. Afterward, she should clean nebulizer and solution chamber according to manufacturer’s recommendations.
WARNING Advise patient not to use more than the recommended dosage of bitolterol; excessive use of sympathomimetic may be fatal.

Tell patient to wait 1 to 3 minutes between metered-dose inhalations.

Category

Chemical class: Hirudin analogue
Therapeutic class: Anticoagulant

Pregnancy category: B

Indications

As adjunct to provide anticoagulation and prevent thrombosis in patients with unstable angina who are having percutaneous transluminal coronary angioplasty or percutaneous coronary intervention

IV

Adults.Initial: Immediately before angioplasty, 0.75-mg/kg bolus; then 1.75 mg/ kg/hr as continuous infusion for duration of procedure. Five min after bolus dose and with continuous infusion running, another 0.3-mg/kg dose may be given if needed. After procedure, 1.75 mg/kg/hr may be given for 4 hr by continuous infusion, followed by 0.2 mg/kg/hr for up to 20 hr if needed.
DOSAGE ADJUSTMENT Infusion dosage possibly reduced to 1 mg/kg/hr for patients with severe renal impairment (glomerular filtration rate of 10 to 29 ml/min) and to 0.25 mg/kg/hr for patients having dialysis. Route Onset Peak Duration I.V. Immediate Unknown 1 hr after end of infusion

Mechanism of Action

Selectively binds to thrombin, including thrombin trapped in established clots. Without thrombin, fibrinogen can’t convert to fibrin and clots can’t form.

Incompatibilities

Don’t mix other in same I.V. line before or during bivalirudin administration. Mixing with alteplase, amiodarone, amphotericin B, chlorpromazine HCL, diazepam, prochlorperazine edisylate, reteplase, streptokinase, or vancomycin HCL can result in haze, particulate formation, or precipitation.

Contraindications

Active major bleeding, hypersensitivity to bivalirudin or its components

Interactions

alteplase, antineoplastics, antithymocyte globulin, heparin, NSAIDs, platelet inhibitors, reteplase, streptokinase, strontium chloride Sr 89,
warfarin: Risk of bleeding porfimer: Possibly decreased efficacy of porfimer photodynamic therapy salicylates: Increased risk of hypoprothrombinemia and bleeding

Side Efect

CNS: Headache, intracranial hemorrhage
CV: Hypotension, thrombosis (with gamma brachytherapy)
EENT: Epistaxis, gingival bleeding
GI: Abdominal cramps, diarrhea, GI or retroperitoneal bleeding, nausea, vomiting
GU: Hematuria, vaginal bleeding
MS: Back pain
RESP: Hemoptysis, hemothorax
SKIN: Ecchymosis
Other: Injection site bleeding, hematoma, or pain bivalirudin 146

Cautions

To reconstitute bivalirudin, add 5 ml sterile water for injection to 250-mg vial and swirl gently until dissolved. For initial infusion, dilute reconstituted vial in 50 ml D5W or normal saline solution to yield 5 mg/ml.

For subsequent low-rate infusion, further dilute reconstituted drug in 500 ml D5W or normal saline solution to final concentration of 0.5 mg/ml.

Expect to give 300 to 325 mg of aspirin P.O. daily during bivalirudin therapy.
WARNING Monitor blood coagulation tests before and regularly during therapy; bleeding is a major bivalirudin risk.
WARNING Monitor patient often for bleeding because there’s no antidote for bivalirudin. If life-threatening bleeding occurs, notify prescriber immediately, stop drug, and monitor APTT and other coagulation tests as ordered. Blood transfusions may be needed. Patients with increased bleeding risk include menstruating women; patients with vascular or organ abnormalities, such as severe uncontrolled hypertension, advanced renal disease, infective endocarditis, dissecting aortic aneurysm, diverticulitis, hemophilia, hepatic disease (especially from deficient vitamin K–dependent clotting factors), inflammatory bowel disease, or peptic ulcer disease; and those with recent stroke, major surgery (including eye, brain, or spinal cord), large vessel or lumbar puncture, organ biopsy, spinal anesthesia, or major bleeding (including intracranial, GI, intraocular, retroperitoneal, or pulmonary bleeding).

If patient is receiving gamma brachytherapy, watch closely for evidence of thrombosis (weak or absent pulse, pallor, pain); use of bivalirudin may increase the risk in these patients.

If possible, avoid I.M. injections of any kind to decrease the risk of bleeding.

Discard any unused portion of drug.

PATIENT SAFTY

Inform patient that bivalirudin is a blood thinner administered only in the hospital.

Urge patient to check her skin for bruising or red spots and to immediately report back or stomach pain, trouble breathing, dizziness, fainting, and unusual bleeding (black, tarry stool; blood in urine; coughing blood; heavy menses; nosebleeds). Drug may need to be stopped.

Encourage patient to reduce the risk of injury while receiving bivalirudin, such as by brushing her teeth gently with a softbristled toothbrush.

Caution patient not to take anti-inflammatories, such as ibuprofen, naproxen, ketoprofen, aspirin, and aspirin-like products, or other blood thinners, such as warfarin, while receiving bivalirudin unless directed.

Category

Chemical class: Endothelin receptor antagonist, pyrimidine derivative
Therapeutic class: Antihypertensive

Pregnancy category: X

Indications

To treat pulmonary arterial hypertension in patients with World Health Organization class III or IV symptoms, to improve exercise ability, and to slow worsening of clinical condition
Adults. Initial: 62.5 mg b.i.d., morning and evening for 4 wk. Maintenance: 125 mg b.i.d., morning and evening.
DOSAGE ADJUSTMENT For adults weighing less than 40 kg (88 lb), maintenance dosage is 62.5 mg b.i.d. morning and evening. For patients who have already received ritonavir for 10 days or more, initial dosage is 62.5 mg once daily or once every other day.

Contraindications

Hypersensitivity to bosentan or its components, concurrent use of cyclosporine or glyburide, pregnancy

Interactions

atorvastatin, lovastatin, simvastatin: Decreased level and efficacy of these cyclosporine, ritonavir: Markedly increased blood bosentan level glyburide: Increased liver enzyme and possibly glucose levels; possibly decreased blood bosentan 147 B level of both (and of other oral antidiabetics metabolized by CYP2C9 or CYP3A4) hormonal contraceptives (oral, injected, implanted): Possibly decreased effects of these ketoconazole and other CYP3A4 inhibitors: Increased bosentan blood level and effects rifampicin: Possibly decreased blood bosentan level tacrolimus: Possibly marked increase in blood bosentan level
warfarin: Increased elimination and decreased blood level of warfarin

Side Efect

CNS: Fatigue, headache
CV: Edema, hypotension, palpitations
EENT: Nasopharyngitis
GI: Elevated liver function test results, hepatic injury, indigestion, liver failure
GU: Decreased sperm count
HEME: Decreased hemoglobin level and hematocrit, thrombocytopenia
SKIN: Flushing, pruritus, rash
Other: Hypersensitivity

Cautions

Before giving bosentan, obtain baseline hemoglobin level and liver function test results, as ordered.
WARNING Because bosentan use may cause major birth defects, make sure female patient of childbearing age has had a negative pregnancy test before giving drug.
WARNING Bosentan may cause risk of serious hepatic injury. Assess patient for evidence of hepatic dysfunction, including abdominal pain, fatigue, fever, jaundice, nausea, and vomiting. Monitor liver function test results every month, as ordered.

Expect dosage to be adjusted or drug stopped if liver function test results become elevated. Expect treatment to be stopped if bilirubin level increases to twice the upper limit of normal (or higher) or if clinical symptoms occur in conjunction with liver function test elevations. Bosentan probably won’t be prescribed for patients with moderate to severe hepatic dysfunction or for those with liver function test levels higher than three times the bosentan 148 Vasoconstriction Pulmonary artery Endothelial cell Vascular smooth- muscle cell ETA receptor ETB receptor ET Bosentan binding to receptor Vasodilation Vasoconstriction Pulmonary artery Endothelial cell Vascular smooth- muscle cell ETA receptor ETB receptor ET Bosentan binding to receptor Vasodilation

Mechanism of Action

Bosentan is an endothelin (ET) receptor antagonist that inhibits the effects of ET, a potent vasoconstrictor. ET, a neurohormone produced by endothelial cells that line blood vessels, normally increases during cardiovascular stress. Patients with pulmonary arterial hypertension have an abnormal increase in serum ET level. ET binds with its receptors, ETA and ETB, which are located on endothelial and vascular smooth-muscle cells. When ET binds with these receptors, it causes vasoconstriction, as shown below left, and such long-term effects as fibrosis and hypertrophy. By binding to ETA and ETB receptors, as shown below right, bosentan blocks the vasoconstrictive effects of ET, causing pulmonary artery vasodilation and decreased pulmonary artery pressure. As a result, the patient experiences increased exercise tolerance and decreased breathlessness. upper limit of normal.

Monitor hemoglobin level 1 and 3 months after start of therapy and every 3 months thereafter, as ordered.

Monitor patient’s response to drug, and evaluate her activity tolerance.

PATIENT SAFTY

WARNING Because major birth defects are associated with bosentan, caution female patient of childbearing age to have a urine or serum pregnancy test monthly during bosentan therapy to verify that she isn’t pregnant. Advise her to notify prescriber immediately if she has a late or missed menstrual period. Instruct her to use a reliable nonhormonal method of contraception because bosentan may decrease effectiveness of hormonal contraceptives.

Urge patient to immediately report evidence of hepatic dysfunction, including yellow skin or eyes, fever, nausea, vomiting, fatigue, and abdominal pain.

Stress the importance of keeping appointments for follow-up testing so that drug’s effects can be evaluated.

Inform patient that bosentan is dispensed only by a special access program set up by the drug’s manufacturer and isn’t available from commercial pharmacies. Advise patient to allow for adequate delivery time when refilling prescription so that she doesn’t run out of drug. Instruct her to review the medication guide that comes with each renewed prescription.

Explain to man that drug may reduce sperm count. Urge him to consult prescriber if he has concerns about fertility.

Category

Chemical class: Bromobenzyl quaternary ammonium compound
Therapeutic class: Class III antiarrhythmic

Pregnancy category: C

Indications

To prevent and treat ventricular fibrillation and treat life-threatening ventricular arrhythmias that don’t respond to firstline antiarrhythmics, such as lidocaine
IV:, I.V.OR
I.M.INJECTION Adults with immediate life-threatening ventricular arrhythmias. Initial: 5 mg/kg, undiluted, by rapid I.V. injection; if ventricular fibrillation persists, 10 mg/kg repeated as often as needed. Continuous suppression: 1 to 2 mg/min or 5 to 10 mg/kg of diluted I.V. solution infused over at least 8 min every 6 hr. Adults with other ventricular arrhythmias.Initial: 5 to 10 mg/kg of diluted I.V. solution infused over at least 8 min, repeated every 1 to 2 hr if arrhythmia continues; or 5 to 10 mg/kg undiluted I.M. injection, repeated every 1 to 2 hr if arrhythmia continues. Maintenance: 5 to 10 mg/kg diluted I.V. solution infused over at least 8 min every 6 hours, 1 to 2 mg/min infused continuously, or 5 to 10 mg/kg undiluted I.M. injection every 6 to 8 hr.
DOSAGE ADJUSTMENT Interval between dosages increased for patients with impaired renal function because bretylium is excreted mainly by kidneys. Children with acute ventricular fibrillation.5 mg/kg I.V. given over 8 to 10 min, followed by 10 mg/kg every 15 to 30 min up to total dose of 30 mg/kg. Maintenance: 5 to 10 mg/kg every 6 hr. Children with other ventricular arrhythmias. 5 to 10 mg/kg every 6 hr. Route Onset Peak Duration I.V. 5–10 min* 6–9 hr 6–24 hr I.M. 20–60 min* 6–9 hr 6–24 hr

Contraindications

Digitalis toxicity, hypersensitivity to bretylium

Interactions

catecholamines (such as dopamine and norepinephrine): Increased vasopressor effects of catecholamines digoxin: Possibly worsened digitalis toxicity

Side Efect

CNS: Anxiety, confusion, dizziness, emotional lability, fever, lethargy, lightheadedness, paranoia, psychosis, syncope, vertigo For suppression of ventricular fibrillation; 20 to 120 min for suppression of ventricular tachycardia.
CV: Angina, arrhythmias (including bradycardia and more frequent PVCs), hypotension, orthostatic hypotension, transient hypertension
EENT: Mild conjunctivitis, nasal stuffiness
GI: Abdominal pain, diarrhea, hiccups, nausea, vomiting
GU: Renal impairment
RESP: Dyspnea
SKIN: Diaphoresis, erythematous macular rash, flushing
Other: Injection site pain

Cautions

WARNING Use bretylium cautiously in patients with severe aortic stenosis or pulmonary hypertension because hypotension may occur.

For I.V. infusion, dilute bretylium and administer at 1 to 2 mg/min.

Dilute bretylium in compatible I.V. solution, such as D5W, dextrose 5% in normal saline solution, dextrose 5% in lactated Ringer’s solution, normal saline solution, 5% sodium bicarbonate, 20% mannitol, 1/6 molar sodium lactate, lactated Ringer’s solution, calcium chloride in D5W, and potassium chloride in D5W.
WARNING Patient may experience hypotension while supine. Have her remain supine until tolerance develops. If supine systolic blood pressure falls below 75 mm Hg, expect to give dopamine or norepinephrine and monitor blood pressure closely because vasopressor effects are increased when these are given together.

Be alert for transient hypertension and increased frequency of arrhythmias because bretylium initially triggers release of norepinephrine. Monitor patient’s ECG tracings and blood pressure continuously, and notify prescriber of changes.

Monitor blood bretylium level. Notify prescriber if level falls outside therapeutic range of 0.5 to 1.5 mcg/ml.

PATIENT SAFTY

Advise patient to immediately report chest pain or pressure, pain at I.V. site, or rash.

Warn patient that she may feel dizzy or light-headed even when lying down. Tell her to stay supine and ask for help when trying to move or sit up. Tell her that this sensation usually subsides in a few days.

Category

Chemical class: Ergot alkaloid derivative
Therapeutic class: Antidiabetic, antidyskinetic, antihyperprolactinemic, dopaminereceptor agonist, growth hormone suppressant, infertility therapy adjunct

Pregnancy category: B

Indications

To treat amenorrhea, galactorrhea, male hypogonadism, and infertility from hyperprolactinemia ,
Adults. Initial: 1.25 to 2.5 mg at bedtime bromocriptine mesylate 150 Norepinephrine Adrenergic nerve terminal Norepinephrine release blocked by bretylium Postsynaptic receptor

Mechanism of Action

Bretylium prolongs the repolarization phase of the action potential and lengthens the effective refractory period, which helps terminate reentry arrhythmias. The drug also acts on adrenergic nerve terminals initially causing early release of norepinephrine, which increases heart rate and blood pressure. Then it blocks release of norepinephrine. This reduces heart rate and blood pressure. Bretylium also increases the ventricular threshold, making the ventricular myocardium less responsive to ectopic impulses and preventing ventricular fibrillation. with snack. Increased by 2.5 mg every 3 to 7 days as needed to a total daily dose of 5 to 7.5 mg given in divided doses with snacks. Maintenance: 2.5 mg b.i.d. or t.i.d. with meals. To treat prolactin-secreting adenoma , Adults and adolescents age 15 and over. Initial: 1.25 mg b.i.d. or t.i.d. with meals. Increased gradually over several weeks, if needed, to 10 to 20 mg daily in divided doses with meals. Some patients may need higher doses. Maintenance: 2.5 to 20 mg daily in divided doses with meals. To treat Parkinson’s disease ,
Adults. Initial: 1.25 mg at bedtime with snack or b.i.d. with meals. Increased by 2.5 mg every 14 to 28 days, if needed. Maintenance: 2.5 to 40 mg daily in divided doses with meals. To treat acromegaly , Adults and children age 15 and over. Initial: 1.25 to 2.5 mg at bedtime with snack for 3 days. Then increased by 1.25 to 2.5 mg every 3 to 7 days, if needed, up to 30 mg daily. Maintenance: Usually 10 to 30 mg daily at bedtime with snack or in divided doses with meals. To control blood glucose level in type 2 diabetes mellitus, with diet and exercise
Adults. Initial: 0.8 mg once daily within 2 hr after waking up in morning. Increased weekly in increments of 0.8 mg, as needed. Maximum: 4.8 mg daily. Route Onset Peak Duration P.O.* 2 hr 8 hr 24 hr P.O. 30–90 min 2 hr Unknown P.O. 1–2 hr 4–8 wk 4–8 hr

Mechanism of Action

Inhibits release of prolactin and growth hormone from the anterior pituitary gland, thus restoring testicular or ovarian function and suppressing lactation. Bromocriptine decreases dopamine turnover in the CNS, depleting dopamine or blocking its receptors in the brain, alleviating dyskinesia.

Contraindications

Breast-feeding; hypersensitivity to bromocriptine, other ergot alkaloids, or their components; ketoacidosis; severe ischemic heart disease or peripheral vascular disease; syncopal migraine; type 1 diabetes mellitus

Interactions

antihypertensives: Increased hypotensive effects clarithromycin, erythromycin, troleandomycin: Increased risk of bromocriptine toxicity CYP3A4 inhibitors: Increased bromocriptine level CYP3A4 inducers: Decreased bromocriptine level dopamine receptor antagonists, including neuroleptic (such as butyrophenones, phenothiazines, or thioxanthenes), metoclopramide: Possibly decreased effectiveness of both ergot alkaloids or derivatives: Increased risk of hypertension haloperidol, loxapine, MAO inhibitors, methyldopa, metoclopramide, molindone, phenothiazines, pimozide, reserpine, risperidone,
thioxanthenes: Increased serum prolactin level, decreased bromocriptine effectiveness levodopa: Additive effects requiring reduced levodopa dose ritonavir: Increased bromocriptine level sympathomimetic : Possibly increased risk of hypertension and tachycardia
alcohol use: Possibly disulfiram-like reaction

Side Efect

CNS: Asthenia, confusion, dizziness, drowsiness, fatigue, hallucinations, headache, light-headedness, syncope
CV: Hypertension, hypotension, orthostatic hypotension, pericarditis, pericardial effusion, Raynaud’s phenomenon
EENT: Amblyopia, dry mouth, nasal congestion, rhinitis, sinusitis
ENDO: Hypoglycemia
GI: Abdominal cramps, anorexia, constipation, diarrhea, GI bleeding, indigestion, nausea, vomiting
RESP: Pleural effusion or thickening, * For amenorrhea, galactorrhea, male hypogonadism, infertility from hyperprolactinemia, and prolactin-secreting adenoma. For Parkinson’s disease. For acromegaly. monary fibrosis
Other: Intense impulse to gamble

Cautions

Use bromocriptine cautiously if patient has a history of psychosis or cardiovascular disease,especially after MI with residual arrhythmia.In severe psychotic disorder, bromocriptine isn’t recommended because it may worsen the disorder or reduce the effects of used to treat it.

Expect to perform a pregnancy test every 4 weeks during the amenorrheic period. Once menses resume, test whenever a period is missed, as ordered.

Plan to withhold bromocriptine if patient becomes pregnant.

If rapidly expanding adenoma needs continued therapy, watch closely for hypertensive crisis.

Bromocriptine shouldn’t be given postpartum if patient has a history of coronary artery disease or other severe cardiovascular problem unless risk of withdrawing drug is greater than risk of use. If so, monitor closely for signs and symptoms of CV dysfunction, such as chest pain.

Expect to give drug with levodopa if patient is being treated for Parkinson’s disease.

Assess for hypotension when bromocriptine therapy starts and hypertension (typically during second week). Monitor blood pressure often if patient takes other antihypertensives.

If patient has a history of peptic ulcer or GI bleeding, watch for new bleeding.

Take safety precautions, such as keeping bed in low position with side rails up, because drug can cause dizziness, drowsiness, light-headedness, and syncope.

PATIENT SAFTY

Tell patient to take each dose with a meal, milk, or a snack to minimize nausea.

Caution patient about possible dizziness, drowsiness, and light-headedness. Urge patient to avoid hazardous activities until drug effects are known.

Advise against sudden position changes to minimize orthostatic hypotension.

Warn patient to avoid alcohol while taking bromocriptine because it may cause disulfiram-like reactions, such as chest pain, confusion, a fast or pounding heartbeat, facial flushing, diaphoresis, nausea, vomiting, a throbbing headache, blurred vision, and severe weakness.

Tell patient to take a missed dose as soon as she remembers it, unless it’s almost time for the next dose. In that case, tell her to wait until the next scheduled dose. Warn her not to double the dose. Advise her to contact prescriber if she misses more than one dose.

Urge patient to report

Side Efect

, such as an unremitting headache, nausea, vomiting, or other signs of CNS toxicity.

Tell patient who takes large doses of bromocriptine to schedule regular dental checkups because the drug can decrease saliva flow, which may encourage dental caries, periodontal disease, oral candidiasis, and discomfort.

Tell patient with acromegaly to keep her fingers warm to prevent cold-sensitive digital vasospasm.

If patient has type 2 diabetes, provide instruction about diet, exercise, effects of hyperglycemia and hypoglycemia, hygiene, foot care, and ways to avoid infection.

Category

Chemical class: Glucocorticoid
Therapeutic class: Antiasthmatic, antiinflammatory

Pregnancy category: B

Indications

To manage symptoms of seasonal or perennial allergic rhinitis NASAL AEROSOL Adults and children over age 6. 64 mcg in each nostril b.i.d. or 128 mcg in each nostril daily. Maximum: 256 mcg daily. Maintenance: Lowest dosage that controls symptoms. NASAL POWDER Adults and children over age 6. 200 mcg in each nostril daily. Maximum: 800 mcg daily (adults and adolescents); 400 mcg daily (children). Maintenance: Lowest dosage that controls symptoms. NASAL SUSPENSION Adults and children over age 6. 32 mcg in each nostril daily. Maximum: 256 mcg daily (adults and adolescents); 128 mcg daily (children). Maintenance: Lowest dosage that controls symptoms. To manage symptoms of perennial nonallergic rhinitis NASAL AEROSOL Adults and adolescents.64 mcg in each nostril b.i.d. or 128 mcg in each nostril daily. Maximum: 256 mcg daily. Maintenance: Lowest dosage that controls symptoms. NASAL POWDER Adults and adolescents. 200 mcg in each nostril daily. Maximum: 800 mcg daily. Maintenance: Lowest dosage that controls symptoms. To provide maintenance therapy in chronic bronchial asthma ORAL INHALATION Adults previously on bronchodilators alone. 1 or 2 inhalations (200 to 400 mcg) b.i.d. Maximum: 800 mcg daily. Adults previously on inhaled corticosteroids. 1 or 2 inhalations (200 to 400 mcg) b.i.d. Maximum: 800 mcg b.i.d. as needed and tolerated. Adults previously on systemic corticosteroids. 2 to 4 inhalations (400 to 800 mcg) b.i.d. Maximum: 1,600 mcg daily. Children age 6 and over. 1 inhalation (200 mcg) b.i.d. Maximum: 400 mcg b.i.d. as needed and tolerated. ORAL INHALATION(PULMICORT FLEXHALER) Adults and adolescents age 18 and over. Initial: 180 or 360 mcg b.i.d., increased as needed. Maximum: 720 mcg b.i.d. Children ages 6 to 17. Initial: 180 or 360 mcg b.i.d. Maximum: 360 mcg b.i.d. To prevent or provide maintenance therapy in chronic bronchial asthma NEBULIZED INHALATION(PULMICORT RESPULES) Children ages 1 to 8 previously on bronchodilators alone. 0.25 mg b.i.d. or 0.5 mg daily by jet nebulizer. Maximum: 0.5 mg/day. Children ages 1 to 8 previously on inhaled steroids. 0.25 mg b.i.d. or 0.5 mg daily inhaled by jet nebulizer. Maximum: 1 mg/day. Children ages 1 to 8 previously on systemic corticosteroids.0.5 mg b.i.d. or 1 mg daily inhaled by jet nebulizer. Maximum: 1 mg/day. To treat mild to moderate active Crohn’s disease involving the ileum, the ascending colon, or both
Adults. 9 mg daily in the morning for 8 wk. To maintain clinical remission of mild to moderate Crohn’s disease involving the ileum, the ascending colon, or both
Adults. 6 mg daily in the morning for up to 3 months.
DOSAGE ADJUSTMENT Dosage reduced for patients with heptic insufficiency and those taking ketoconazole or other CYP3A4 inhibitor. Route Onset Peak Duration Nasal 10 hr– 3 days– Unknown aerosol 3 days 3 wk Nasal In 4 wk Unknown Unknown powder or suspension Oral In 4 wk Unknown Unknown inhalation Nebulized 2–8 days 4–6 wk Unknown inhalation P.O. Unknown 30 min– Unknown (capsules) 10 hr

Mechanism of Action

Inhibits inflammatory cells and mediators, possibly by decreasing influx into nasal passages or bronchial walls. As a result, nasal or airway inflammation decreases. Oral inhalation form also inhibits mucus secretion in airways, decreasing the amount and viscosity of sputum.

Contraindications

Hypersensitivity to budesonide or its components, recent septal ulcers or nasal surgery or trauma (
NASAL SPRAY); status asthmaticus or other acute asthma episodes (oral inhalation)

Interactions

clarithromycin, erythromycin, itraconazole, ketoconazole, other CYP3A4 inhibitors: Possibly increased blood budesonide level

Side Efect

CNS: Amnesia, asthenia, benign intracranial hypertension, dizziness, fatigue, fever, headache
EENT: Bad taste, cataracts, dry mouth, epistaxis, glaucoma, nasal irritation, oral or pharyngeal candidiasis, pharyngitis, rhinitis, sinusitis
ENDO: Growth suppression in children
GI: Abdominal pain, diarrhea, dyspepsia, flatulence, indigestion, nausea, vomiting
GU: UTI
MS: Arthralgia, back pain
RESP: Bronchospasm, increased cough, respiratory tract infection
SKIN: Contact dermatitis, purpura, rash, urticaria
Other: Anaphylaxis, angioedema

Cautions

Use budesonide cautiously if patient has tubercular infection; untreated fungal, bacterial, or systemic viral infection; or ocular herpes simplex.

Closely monitor a child’s growth pattern; budesonide may stunt growth.
WARNING Assess patient who switches from a systemic corticosteroid to inhaled budesonide for adrenal insufficiency (fatigue, hypotension, lassitude, nausea, vomiting, weakness), which may be life-threatening. Hypothalamic-pituitary-adrenal axis function may take several months to recover after stopping systemic corticosteroids. Stopping budesonide abruptly may cause adrenal insufficiency.

Administer Respules by jet nebulizer connected to an air compressor.

Patient exposed to chickenpox may receive varicella zoster immune globulin or pooled I.V. immunoglobulin. If chickenpox develops, give antiviral as ordered. A patient exposed to measles may need pooled I.M. immunoglobulin.

Assess patient for effectiveness of budesonide therapy, especially if being weaned from a systemic corticosteroid. If patient has increased asthma or an immunologic condition previously suppressed by systemic corticosteroid—such as rhinitis, conjunctivitis, an eosinophilic condition, eczema, or arthritis—notify prescriber.

Pulmicort Flexhaler contains small amounts of lactose, which may trigger coughing, wheezing, or bronchospasm in a patient with a severe milk-protein allergy.

Monitor patient for evidence of hypersensitivity, such as contact dermatitis, rash, urticaria, angioedema, bronchospasm, or anaphylaxis. If present, notify prescriber immediately. Expect to stop budesonide and provide emergency supportive care.

PATIENT SAFTY

Urge patient taking oral capsules to swallow them whole and not to chew or break them.

Instruct patient who uses
NASAL SPRAY to shake container before each use. Instruct her to blow her nose, tilt her head slightly forward, and insert tube into a nostril, pointing toward inner corner of eye, away from nasal septum. Tell her to hold the other nostril closed and spray while inhaling gently. Then have her repeat in the other nostril.

Instruct patient to prime oral inhaler before using it for first time by holding canister upright with mouthpiece on top and twisting base of device fully to right and then fully to left until it clicks. Teach her to load each each dose just before use in the same way. After loading a dose, caution patient not to shake device or blow into it. Tell patient to turn her head away from device and exhale. Then have her hold device upright, place her lips around mouthpiece, and inhale deeply. Device will discharge a dose. Tell patient to remove her lips from mouthpiece to exhale.

Caution patient not to use an oral inhaler with a spacer device.

Advise patient to rinse her mouth with water after each dose and to spit the water out. Tell her to contact her prescriber if she develops a mouth or throat infection.

Instruct patient not to use budesonide as a rescue inhaler.

Tell patient to contact prescriber if symptoms persist or have worsened after 3 weeks. Caution against increasing the dose on her own.

Inform parents of small children using nebulized Respules that improvement may begin within 2 to 8 days but that full effect may not be evident for 4 to 6 weeks.

Caution patient to avoid exposure to chickenpox and measles and, if exposed, to contact prescriber immediately.

Caution against stopping drug abruptly.

Instruct patient on long-term therapy to have regular eye examinations.

Urge female patient to notify prescriber if she is or could be pregnant.

Category

Chemical class: Sulfonamide derivative
Therapeutic class: Loop diuretic

Pregnancy category: C

Indications

To treat edema caused by heart failure, hepatic disease, and renal disease, including nephrotic syndrome
Adults. 0.5 to 2 mg daily, increased as needed, with a second or third dose every 4 to 5 hr or 0.5 to 2 mg every other day or daily for 3 or 4 days each week. Maximum: 10 mg daily.
IV:, I.V.OR
I.V.INJECTION
Adults. 0.5 to 1 mg over 1 to 2 min daily, increased p.r.n. with a second or third dose every 2 to 3 hr. Maximum: 10 mg daily.
DOSAGE ADJUSTMENT In patients with severe chronic renal insufficiency, continuous infusion (12 mg over 12 hr) may be more effective and less toxic than intermittent infusion. Route Onset Peak Duration P.O. 30–60 min 1–2 hr 4–6 hr I.V. In min 15–30 min 3.5–4 hr

Mechanism of Action

Inhibits reabsorption of sodium, chloride, and water in the ascending limb of the loop of Henle, which promotes their excretion and reduces fluid volume.

Contraindications

Anuria, hepatic coma, hypersensitivity to bumetanide or its components, severe electrolyte depletion

Interactions

aminoglycosides: Increased risk of ototoxicity antihypertensives: Increased hypotensive effect indomethacin: Slowed increase in urine and sodium excretion, inhibited plasma renin activity lithium: Reduced lithium renal clearance, increased risk of lithium toxicity probenecid: Reduced sodium excretion

Side Efect

CNS: Dizziness, encephalopathy, headache
CV: Hypotension
EENT: Ototoxicity
ENDO: Hyperglycemia
GI: Nausea
GU: Azotemia, elevated serum creatinine level
MS: Muscle spasms
Other: Hyperuricemia, hypocalcemia, hypochloremia, hypokalemia, hyponatremia, hypovolemia

Cautions

WARNING A patient hypersensitive to sulfonamides may be hypersensitive to bumetanide. Monitor such a patient closely when starting therapy.

Expect to use parenteral route for patients with impaired GI absorption or in whom the oral route isn’t practical. Switch to oral route, as prescribed, as soon as possible.

Discard unused parenteral solution 24 hours after preparation.

Assess fluid and electrolyte balance closely because bumetanide is a potent diuretic (40 to 60 times more potent than furosemide). Monitor fluid intake and output once every 8 hours, evaluate serum electrolyte levels when ordered, and assess for imbalances.
WARNING Be aware that high-dose or toofrequent administration can cause profound diuresis and water and electrolyte depletion, especially in elderly patients.

Monitor serum potassium level regularly to check for hypokalemia, especially if patient takes a digitalis glycoside for heart failure or has hepatic cirrhosis, ascites, aldosteronism, potassium-losing nephropathy, diarrhea, or a history of ventricular arrhythmias.

Assess for evidence of ototoxicity, such as tinnitus, daily. Rarely, drug may cause ototoxicity, especially with I.V. use, high doses, and increased frequency of dosing in a patient with renal impairment.

Monitor results of renal function tests during therapy to detect

Side Efect

.

PATIENT SAFTY

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Stress importance of monitoring fluid intake and output and watching for evidence of electrolyte imbalance, such as dizziness, headache, and muscle spasms.

Review

Side Efect

, and tell patient to report severe or persistent reactions.

Review potassium-rich , and urge patient to include them in her daily diet.

Urge patient to return for appropriate follow-up care, especially if she’s receiving bumetanide for a chronic condition.

Tell diabetic patient to monitor blood glucose level regularly and to notify prescriber about persistent hyperglycemia.
<3>Chemical class: Opioid, thebaine derivative
Therapeutic class: Opioid analgesic

Pregnancy category: C

Controlled substance schedule: V

Indications

To control moderate to severe pain I.V.OR
I.M.INJECTION Adults and children age 12 and over. 0.3 mg every 6 hr or more, p.r.n. A second 0.3-mg dose given 30 to 60 min after first dose, if needed.
DOSAGE ADJUSTMENT In patients not at high risk for opioid toxicity, I.M. dose increased to 0.6 mg or frequency increased to every 4 hr, if needed, depending on pain severity and patient response. I.V. or I.M. dose reduced by half in elderly or debilitated patients and those who have respiratory disease or also use another CNS depressant. Children ages 2 to 12. 0.002 to 0.006 mg/ kg every 4 to 6 hr, p.r.n. To treat opioid dependence SUBLINGUAL
Adults. 12 to 16 mg daily.

Mechanism of Action

May bind with CNS receptors to alter the perception of and emotional response to pain. Buprenorphine may act by displacing narcotic agonists from their binding sites and competitively inhibiting their actions.

Incompatibilities

Don’t give I.V. buprenorphine through the same I.V. line as diazepam or lorazepam.

Contraindications

Hypersensitivity to buprenorphine or its components Route Onset Peak Duration I.V. Under Under 6–10 hr* 15 min 1 hr I.M. 15 min 1 hr 6–10 hr*

Interactions

CNS depressants,
MAO inhibitors: Additive hypotensive and respiratory and CNS depressant effects of these opioid analgesics: Reduced therapeutic effects if buprenorphine is given before another opioid analgesic

Side Efect

CNS: Dizziness, headache, sedation, vertigo
CV: Bradycardia, hypertension, hypotension
EENT: Miosis
GI: Nausea, vomiting
RESP: Bronchospasm, hypoventilation
SKIN: Diaphoresis, pruritus, rash, urticaria
Other: Anaphylaxis; angioedema; injection site pain, redness, and swelling

Cautions

Use buprenorphine cautiously in patients with severe hepatic or renal impairment, myxedema, hypothyroidism, adrenal insufficiency, CNS depression, coma, toxic psychosis, prostatic hypertrophy, urethral stricture, acute alcoholism, alcohol withdrawal syndrome, kyphoscoliosis, or biliary tract dysfunction. Also use cautiously in patients who take a drug that decreases hepatic clearance, are known drug abusers, or have been addicted to opioids.

Use drug cautiously in patients with head injury, intracranial lesions, or other conditions that could increase CSF pressure.

To avoid causing withdrawal, drug shouldn’t be given for opioid dependence until signs of withdrawal occur.

Give I.V. form over at least 2 minutes.

Inspect injection site for local reactions; don’t use the same site twice.

Monitor vital signs and response to drug often, especially after giving first dose.

PATIENT SAFTY

Instruct patient taking sublingual form to buprenorphine hydrochloride 156 * 4 to 5 hr in children ages 2 to 12. place tablets under her tongue until they dissolve. If patient takes more than two tablets per dose, tell her to place all tablets under her tongue at the same time. If they won’t fit, tell her to place two at a time under her tongue until full dose has dissolved. Caution against swallowing tablets.

Category

Chemical class: Aminoketone derivative
Therapeutic class: Antidepressant, smoking cessation adjunct

Pregnancy category: C

Indications

To treat depression (WELLBUTRIN SR)
Adults. Initial: 150 mg daily in morning for 3 days; then 150 mg b.i.d. and, after several wk, 200 mg b.i.d., as needed and tolerated. Maximum: 400 mg daily or 200 mg/dose. (WELLBUTRIN XL)
Adults. Initial: 150 mg daily in morning for at least 3 days; then 300 mg daily and, after 4 wk, 450 mg daily, as needed and tolerated. Maximum: 450 mg daily. (APLENZIN)
Adults. Initial: 174 mg daily in the morning for 3 days. Then, if tolerated well, dosage increased to 348 mg daily in the morning. After 4 wk of therapy, dosage increased to 522 mg daily in the morning, if needed.
Adults. Initial: 100 mg b.i.d., increased after 3 or more days to 100 mg t.i.d., as needed. Maximum: 450 mg daily or 150 mg/dose. To aid in smoking cessation
Adults.Initial: 150 mg daily for 3 days and then 150 mg b.i.d. for 7 to 12 wk. Maximum: 300 mg daily or 150 mg/dose. To prevent seasonal major depressive episodes in patient with seasonal affective disorder
Adults.Initial: 150 mg once daily in morning starting in autumn, increased after 1 wk to 300 mg once daily in morning, if tolerated and needed. Decreased to 150 mg once daily 2 wk before stopping in early spring.
DOSAGE ADJUSTMENT For patients with severe hepatic cirrhosis, no more than 75 mg daily of Wellbutrin, 100 mg daily or 150 mg every other day of Wellbutrin SR, 150 mg every other day of Wellbutrin XL or Zyban, and 174 mg every other day of Aplenzin. In renal impairment, dosage or frequency decreased on an individual basis. Route Onset Peak Duration P.O. 1–3 wk Unknown Unknown

Mechanism of Action

May inhibit norepinephrine, serotonin, and dopamine uptake by neurons, which significantly relieves evidence of depression.

Contraindications

Anorexia, bulimia, use of another form of bupropion, hypersensitivity to bupropion or its components, seizure disorder, treatment requiring abrupt discontinuation of alcohol or sedatives (including benzodiazepines), use within 14 days of an MAO inhibitor

Interactions

amantadine, levodopa: Increased adverse reactions to bupropion carbamazepine, cimetidine, phenobarbital,
phenytoin: Increased bupropion metabolism clozapine, fluoxetine, haloperidol, lithium, loxapine, maprotiline, molindone, phenothiazines, thioxanthenes, trazodone, tricyclic antidepressants: Increased risk of major motor seizures levodopa: Increased adverse bupropion effects
MAO inhibitors: Increased risk of acute bupropion toxicity nicotine: Possibly increased blood pressure
warfarin: Possibly altered PT and INR; risk of hemorrhagic or thrombotic complications alcohol use, recreational drug abuse: Lowered seizure threshold

Side Efect

CNS: Agitation, akathisia, anxiety, asthenia, CNS stimulation, coma, confusion, decreased concentration or memory, delusions, depression, dizziness, euphoria, fever, general or migraine headache, hallucinations, hostility, insomnia, irritability, mania, nervousness, paranoia, paresthesia, seizures, sleep disorder, somnolence, stroke, suicidal ideation, syncope, tremor, vertigo
CV: Arrhythmias, chest pain, complete AV block, hypertension, MI, orthostatic hypotension, palpitations, phlebitis, tachycardia, vasodilation
EENT: Altered taste, amblyopia, blurred vision, dry mouth, hearing loss, increased ocular pressure, pharyngitis, sinusitis, taste perversion, tinnitus
ENDO: Hyperglycemia, hypoglycemia, syndrome of inappropriate ADH secretion
GI: Abdominal pain, anorexia, constipation, diarrhea, dysphagia, flatulence, GI hemorrhage, GI ulceration, hepatitis, increased appetite, intestinal perforation, nausea, pancreatitis, vomiting
GU: Urinary frequency and urgency, UTI, vaginal hemorrhage
HEME: Anemia, leukocytosis, leukopenia, lymphadenopathy, pancytopenia, thrombocytopenia
MS: Arthralgia, arthritis, muscle twitching, myalgia, rhabdomyolysis
RESP: Bronchospasm, cough, pulmonary embolism
SKIN: Diaphoresis, exfoliative dermatitis, flushing, pruritus, rash, urticaria
Other: Angioedema, generalized pain, hot flashes, infection, serum sicknesslike reaction, weight loss

Cautions

Use cautiously in patients with renal impairment; drug is excreted by kidneys.

Monitor children, adolescents, and depressed patients closely for worsened depression and increased suicide risk, especially when therapy starts or dosage changes.

If patient takes bupropion for smoking cessation, watch for neuropsychiatric symptoms, including changes in behavior, hostility, agitation, depressed mood, suicidal ideation, and worsening of psychiatric illness. If present, notify prescriber immediately, begin safety measures, and expect to discontinue drug.

To reduce seizure risk, allow at least 4 hours (tablets) or 8 hours ( tablets) between doses.

Use seizure precautions, especially in patients who take OTC stimulants or anorectics; use excessive alcohol or sedatives; are addicted to opioids, cocaine, or stimulants; take that lower the seizure threshold; have a history of seizures, head trauma, or CNS tumors; have severe hepatic cirrhosis; or take insulin or an oral antidiabetic.

Using transdermal nicotine with bupropion may cause hypertension. Watch closely.

PATIENT SAFTY

Advise patient to take bupropion for 7 or more days before stopping smoking.

Tell patient to swallow tablets whole and not to cut, crush, or chew them.

Tell patient to take bupropion with food.

Urge patient to avoid or minimize consuming alcohol and sedatives during therapy and not to stop drug abruptly because seizures may occur.

Urge caregivers to monitor depressed patient closely for worsened depression, especially when therapy starts or dosage changes.

If patient takes bupropion for smoking cessation, explain that it may cause serious adverse effects, including changes in behavior, hostility, agitation, depressed mood, suicidal ideation, and worsening of psychiatric illness. If present, patient should notify prescriber immediately and expect to discontinue drug.

Category

Chemical class: Azaspirodecanedione
Therapeutic class: Antianxiety

Pregnancy category: B

Indications

To manage anxiety
Adults. Initial: 5 mg t.i.d. or 7.5 mg b.i.d. buspirone hydrochloride 158 increased by 5 mg daily at 2to 3-day intervals until desired response occurs. Maintenance: 20 to 30 mg daily (usual therapeutic range). Maximum: 60 mg daily.
DOSAGE ADJUSTMENT When used with nefazodone, dosage as little as 2.5 mg daily. Route Onset Peak Duration P.O. 1–4 wk 3–6 wk Unknown

Mechanism of Action

May act as a partial agonist at serotonin 5hydroxytryptamine1Areceptors in the brain, producing antianxiety effects.

Contraindications

Hypersensitivity to buspirone or its components, severe hepatic or renal impairment

Interactions

diltiazem, erythromycin, itraconazole, nefazodone, nordiazepam, verapamil: Increased blood level and adverse effects of buspirone
haloperidol: Increased haloperidol level hepatic enzyme CYP3A4 inducers, such as dexamethasone and certain anticonvulsants (phenytoin, phenobarbital, carbamazepine): Possibly increased rate of buspirone metabolism hepatic enzyme CYP3A4 inhibitors, such as ketoconazole and ritonavir: Possibly inhibited buspirone metabolism and increased blood level
MAO inhibitors: Increased risk of hypertension
rifampin: Decreased blood buspirone level and pharmacodynamic effects food: Possibly decreased buspirone clearance grapefruit juice: Increased blood buspirone level

Side Efect

CNS: Akathisia, anger, ataxia, cogwheel rigidity, confusion, decreased concentration, depression, dizziness, dream disturbances, drowsiness, dyskinesias, dystonia, excitement, extrapyramidal symptoms, fatigue, headache, hostility, insomnia, lack of coordination, light-headedness, mood swings, nervousness, paresthesia, parkinsonism, restless leg syndrome, restlessness, serotonin syndrome, transient recall impairment, tremor, weakness
CV: Chest pain, palpitations, tachycardia
EENT: Blurred vision, dry mouth, nasal congestion, pharyngitis, tinnitus, tunnel vision
GI: Abdominal or gastric distress, constipation, diarrhea, nausea, vomiting
GU: Urine retention
MS: Myalgia
SKIN: Diaphoresis, ecchymosis, rash, urticaria
Other: Angioedema

Cautions

Use buspirone cautiously in patients with hepatic or renal impairment.

Institute safety precautions because of possible adverse CNS reactions.

Follow closely if patient is being withdrawn from long-term therapy with benzodiazepines or other sedative-hypnotic while starting buspirone because buspirone won’t prevent withdrawal symptoms.

PATIENT SAFTY

Advise patient to take buspirone consistently, either always with or always without food.

Caution patient to avoid drinking large amounts of grapefruit juice.

Inform patient that 1 to 2 weeks of therapy may be needed before she notices drug’s antianxiety effect.

Stress the importance of not taking more buspirone than prescribed.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Category

Chemical class: Barbiturate
Therapeutic class: Sedative-hypnotic

Pregnancy category: D

Controlled substance schedule: III

Indications

To provide daytime sedation ELIXIR,
Adults.15 to 30 mg t.i.d. or q.i.d. To treat insomnia ELIXIR,
Adults.50 to 100 mg every at bedtime. To provide preoperative sedation ELIXIR,
Adults.50 to 100 mg 60 to 90 min before surgery. Children.2 to 6 mg/kg. Maximum: 100 mg/ dose.
DOSAGE ADJUSTMENT Dosage reduced in patients with impaired renal or hepatic function and in elderly or debilitated patients because they may be more sensitive to drug. Route Onset Peak Duration P.O. 45–60 min Unknown 6–8 hr

Mechanism of Action

Inhibits the upward conduction of nerve impulses in the brain’s reticular formation, which disrupts impulse transmission to the cortex. As a result, butabarbital depresses the CNS and produces drowsiness, sedation, and hypnosis.

Contraindications

History of addiction to sedative or hypnotic drug, hypersensitivity to butabarbital or its components, porphyria, severe hepatic or respiratory disease

Interactions

acetaminophen: Increased risk of hepatotoxicity (with large doses of or long-term therapy with butabarbital) activated charcoal: Reduced butabarbital absorption carbamazepine: Decreased blood carbamazepine level chloramphenicol, corticosteroids, digitalis glycosides: Increased metabolism and decreased effects of these clonazepam: Increased clearance and reduced efficacy of clonazepam CNS depressants, including OTC sedatives and hypnotics: Additive CNS depression doxycycline: Shortened half-life and decreased effects of doxycycline fenoprofen: Reduced bioavailability and effects of fenoprofen griseofulvin: Reduced griseofulvin absorption hydantoins, such as
phenytoin: Unpredictable effects on barbiturate metabolism
MAO inhibitors: Prolonged barbiturate effects meperidine: Prolonged CNS depressant effects of meperidine methadone: Reduced methadone actions
methoxyflurane: Increased risk of nephrotoxicity metronidazole: Decreased antimicrobial effect of metronidazole oral anticoagulants: Decreased anticoagulant effect oral contraceptives with estrogen: Decreased contraceptive effect phenylbutazone: Reduced elimination halflife of phenylbutazone
rifampin: Decreased butabarbital effectiveness sodium valproate,
valproic acid: Decreased butabarbital metabolism and increased adverse CNS effects
theophylline: Decreased blood level and effects of theophylline
alcohol use: Additive CNS depression

Side Efect

CNS: Agitation, anxiety, ataxia, clumsiness, CNS depression, confusion, depression, dizziness, drowsiness, fever, hallucinations, headache, hyperkinesia, insomnia, irritability, nervousness, nightmares, psychiatric disturbance, sleep driving (see Patient Teaching section), somnolence, syncope
CV: Hypertension
EENT: Laryngospasm
GI: Constipation, hepatic dysfunction, nausea, vomiting
MS: Rickets
RESP: Apnea, bronchospasm, respiratory depression
SKIN: Exfoliative dermatitis, StevensJohnson syndrome
Other: Anaphylaxis, angioedema, drug tolerance, physical and psychological dependence

Cautions

Use butabarbital cautiously, if at all, in patients with depression, suicidal tendency, history of drug abuse, or hepatic dysfunction. Don’t administer drug to patients with premonitory signs of hepatic coma.
WARNING Monitor patient closely following butabarbital ingestion because anaphylaxis butabarbital sodium 160 or angioedema, although rare, may occur with first dose or later doses. Notify prescriber immediately, and provide supportive emergency care.

Expect to give drug for no more than 2 weeks to treat insomnia because, like all barbiturates, it loses effectiveness for sleep induction and sleep maintenance after 2 weeks.

Monitor butabarbital intake closely during long-term use because tolerance and psychological and physical dependence may develop.

Avoid abrupt withdrawal of butabarbital to prevent withdrawal symptoms.

Monitor elderly and debilitated patients closely because drug may cause marked excitement, depression, and confusion in these patients.

If patient experiencing pain receives butabarbital, monitor closely for paradoxical excitement.

If pregnant woman took butabarbital during last trimester, monitor infant for withdrawal symptoms.

Monitor patient for worsening of insomnia or emergence of abnormal thinking or behavior during therapy. If butabarbital unmasks them, patient will need further assessment.

PATIENT SAFTY

Stress the importance of taking butabarbital exactly as prescribed because it can be addictive. Warn against increasing the dose or decreasing the dosage interval without consulting prescriber.

Advise patient to notify prescriber if insomnia persists after 7 days of butabarbital therapy.

Tell patient to avoid alcohol and OTC sedatives and hypnotics during butabarbital therapy because of additive CNS effects.

Advise patient to avoid hazardous activities until butabarbital’s CNS effects are known.

Advise female patient not to rely on oral contraceptives during butabarbital therapy.

Explain that butabarbital may cause sleep driving, in which the patient drives while not fully awake and typically cannot recall doing so. Tell family members to report any episodes of sleep driving.

Category

Chemical class: Opioid
Therapeutic class: Anesthesia adjunct, opioid analgesic

Pregnancy category: C

Controlled substance schedule: II

Indications

To manage pain
I.V.INJECTION
Adults.0.5 to 2 mg (usually 1 mg) every 3 to 4 hr, as needed.
I.M.INJECTION
Adults.1 to 4 mg (usually 2 mg) every 3 to 4 hr, as needed. Maximum: 4 mg/single dose. NASAL INHALATION
Adults. 1 spray (1 mg) in one nostril. Dose repeated after 60 to 90 min; two-dose sequence repeated every 3 to 4 hr, as needed. For severe pain, 2 sprays (1 in each nostril) every 3 to 4 hr, as needed.
DOSAGE ADJUSTMENT Dose reduced to 1 spray in one nostril for elderly patients and those with impaired hepatic or renal function. Dose repeated after 90 to 120 min; two-dose sequence repeated every 6 hr or more, as needed. As adjunct to provide preoperative anesthesia I.V.OR
I.M.INJECTION
Adults. Individualized. Average: 2 mg 60 to 90 min before surgery. As adjunct to provide anesthesia
I.V.INJECTION
Adults. Individualized. Average: 1 to 4 mg and then supplemental doses of 0.5 to 1 mg, p.r.n. Total usually required during surgery is 60 to 180 mcg/kg.
DOSAGE ADJUSTMENTPaarenteral doses reduced by half for elderly patients and patients with impaired hepatic or renal function.

Mechanism of Action

Binds with specific CNS receptors to alter the perception of and emotional response to pain.

Contraindications

Hypersensitivity to butorphanol or its components (including the preservative benzethonium chloride) Route Onset Peak Duration I.V. 2–3 min 30 min 2–4 hr I.M. 10–30 min 30–60 min 3–4 hr InhalationIn 15 min 1–2 hr 4–5 hr

Interactions

CNS depressants: Additive CNS depression nasal vasoconstrictors, such as oxymetazoline: Decreased absorption rate and delayed onset of butorphanol
alcohol use: Additive CNS depression

Side Efect

CNS: Anxiety, confusion, difficulty making purposeful movements, difficulty speaking, dizziness, euphoria, floating feeling, headache, insomnia (with nasal form), lethargy, nervousness, paresthesia, sensation of heat, somnolence, syncope, tremor, vertigo
CV: Chest pain, hypotension, palpitations, tachycardia, vasodilation
EENT: Blurred vision, dry mouth, ear pain, epistaxis, nasal congestion or irritation (with nasal form), pharyngitis, rhinitis, sinus congestion, sinusitis, tinnitus, unpleasant taste
GI: Anorexia, constipation, epigastric pain, nausea, vomiting
RESP: Apnea, bronchitis, cough, dyspnea, respiratory depression, shallow breathing, upper respiratory tract infection
SKIN: Clammy skin, pruritus

Cautions

Use butorphanol cautiously, if at all, in patients with depression, suicidal tendency, history of drug abuse, or hepatic or renal dysfunction.

Because drug can raise CSF pressure, use it cautiously, if at all, in patients with head injury. Because it can increase cardiac workload, use with extreme caution in patients with acute MI, ventricular dysfunction, or coronary insufficiency.

Be aware that butorphanol has a high potential for abuse.

Monitor patient after first dose of nasal form; hypotension and syncope may occur.

Take safety precautions because butorphanol causes CNS depression.

Assess respiratory status closely because drug causes respiratory depression.

Monitor blood pressure often after giving drug. If severe hypertension develops (rare), stop drug at once and notify prescriber. If patient isn’t narcotic-dependent, expect to administer naloxone to reverse butorphanol’s effects.

PATIENT SAFTY

Stress the importance of taking butorphanol exactly as prescribed because it can be addictive. Warn patient not to increase the dose or decrease the dosage interval without consulting prescriber.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Tell patient to avoid alcohol and other CNS depressants, including OTC , while taking butorphanol because of additive adverse CNS reactions.

Teach patient how to use nasal form properly by giving these instructions: After blowing nose to clear the nostrils, pull clear cover from the pump unit and remove protective clip from its neck. Prime pump unit by placing the nozzle between first and second fingers with thumb on the bottom of the bottle. Then pump sprayer unit firmly and quickly until a fine spray appears (7 or 8 strokes). Insert spray tip about 1 cm (one-third inch) into one nostril, pointing tip toward the back of the nose. Close other nostril with one finger and tilt head slightly forward. Then pump sprayer firmly and quickly by pushing down on the pump unit’s finger grips and against the thumb at the bottom of the bottle. Sniff gently with mouth closed. After spraying, remove pump from nose, tilt head back, and sniff gently for a few more seconds. Then replace protective clip and clear cover.

Category

Chemical class: Glycoprotein
Therapeutic class: Human plasma C1 esterase inhibitor replacement

Pregnancy category: C

Indications

To treat acute abdominal or facial attacks of hereditary angioedema
I.V.INJECTION Adults and adolescents.20 units/kg given at 4 ml/min.

Mechanism of Action

Suppresses activation of the contact system that may mediate increased vascular permeability and evidence of hereditary angioedema by inactivating plasma kallikrein and factor XIIa, which prevents generation of bradykinin. Patients with hereditary angioedema have low levels of endogenous or functional C1 esterase inhibitor, a normal constituent of plasma. By increasing these levels, the contact system becomes sufficiently inactivated to relieve signs and symptoms.

Incompatibilities

Do not mix C1 esterase inhibitor with other or solutions. Administer by a separate infusion line.

Contraindications

Hypersensitivity (including anaphylaxis) to C1 esterase inhibitor preparation or its components

Interactions

anticoagulants, thrombolytics: Possibly decreased effectiveness

Side Efect

CNS: Chills, fever, headache
CV: Thrombosis
EENT: Laryngeal edema, laryngospasm, nasopharyngitis, taste abnormality
GI: Abdominal pain, diarrhea, nausea, vomiting
MS: Back pain, muscle spasm
Other: Anaphylaxis, facial or generalized pain, injection site pain and redness, shock, swelling in area of shoulder and chest, worsening of hereditary angioedema

Cautions

Reconstitute C1 esterase inhibitor using the Mix2Vial transfer set or a doubleended needle and vented filter spike. After cleaning tops of drug and diluent vials with alcohol and letting them dry, grip the Mix2Vial transfer set together with the clear package (after peeling away the lid) and snap blue end of transfer set onto diluent vial stopper at a 90-degree angle. Carefully remove clear package from transfer set. With drug vial sitting on a flat surface, invert diluent vial with transfer set attached and snap transparent adapter onto drug vial stopper at a 90-degree angle. Gently swirl drug vial to fully dissolve. Do not shake vial. Once drug is dissolved, grasp drug side of transfer set and, with the other hand, grasp blue diluent side of transfer set to unscrew set into two pieces. Draw air into an empty, sterile syringe. With drug vial upright, screw syringe to transfer set and inject air. Invert system upside down while keeping syringe plunger pressed, and draw concentrate into syringe by pulling plunger back slowly. Then unscrew syringe from transfer set keeping plunger of syringe facing down.

Attach filled syringe to an I.V. administration set and infuse 4 ml/minute within 8 hours after reconstitution. Do not refrigerate or freeze reconstituted solution.

If patient needs more than one vial, contents of multiple vials may be pooled in a single administration device, using a new unused Mix2Vial transfer set for each drug vial.

Do not give C1 esterase inhibitor with any other drug. Administer it using a separate infusion line.

Store C1 esterase inhibitor in its original carton to protect from light. Do not freeze.
WARNING Severe hypersensitivity reactions may occur with signs and symptoms for hereditary angioedema. Monitor patient C closely for evidence of anaphylaxis, generalized urticaria, hives, hypotension, tightness of chest, or wheezing. Discontinue C1 esterase inhibitor immediately and provide supportive care, including epinephrine, as prescribed.

Thrombotic events may occur, especially when higher-than-recommended doses are given or drug is given for off-label uses.

Monitor patient for evidence of infection because C1 esterase inhibitor is extracted from human blood. Although safeguards are used, the potential exists for an infectious agent to be transmitted. Reports of acute hepatitis C have been documented after giving C1 esterase inhibitor.

PATIENT SAFTY

Stress importance of reporting new or persistent signs and symptoms during and after C1 esterase inhibitor therapy.

Inform patient about the potential for pain, such as back pain or muscle spasms, and reassure patient that comfort measures will be provided.

Category

Chemical class: Ergot alkaloid derivative
Therapeutic class: Antihyperprolactinemic

Pregnancy category: B

Indications

To treat idiopathic or adenoma-induced hyperprolactinemic disorders
Adults. 0.25 mg twice/wk. Increased by 0.25 mg/wk at 4-wk intervals, if needed, up to 1 mg twice/wk. Route Onset Peak Duration P.O. Unknown 48 hr Up to 14 days

Mechanism of Action

Binds with dopamine D2receptors to block prolactin synthesis and secretion by the anterior pituitary gland, thereby reducing the serum prolactin level.

Contraindications

History of pulmonary, pericardial, cardiac valvular, or retroperitoneal fibrotic disorders; hypersensitivity to cabergoline, ergot derivatives, or their components; uncontrolled hypertension

Interactions

antihypertensives: Increased risk of hypotension dopamine antagonists (butyrophenones, metoclopramide, phenothiazines, or thioxanthenes): Decreased cabergoline effectiveness

Side Efect

CNS: Aggression, asthenia, depression, fatigue, headache, nervousness, paresthesia, pathological gambling behavior, somnolence, psychotic disorder, vertigo
CV: Orthostatic hypotension, valvulopathy
EENT: Dry mouth
ENDO: Breast pain
GI: Abdominal pain, constipation, diarrhea, flatulence, indigestion, nausea, vomiting
GU: Dysmenorrhea, increased libido
RESP: Pulmonary effusion or fibrosis
SKIN: Alopecia

Cautions

Before each dose increase, check serum prolactin level to assess cabergoline’s effectiveness.

If patient has moderate to severe hepatic impairment, monitor closely for adverse reactions because of decreased cabergoline metabolism.

Expect patient who takes cabergoline long-term to undergo periodic reassessment of cardiac status, including echocardiography, because valvulopathy can occur with prolonged cabergoline use.

Erythrocyte sedimentation rate may increase in a patient with pleural effusion or pleural fibrosis.
WARNING If you detect evidence of overdose, such as syncope, hallucinations, lightheadedness, tachycardia, and nasal congestion, notify prescriber and treat as ordered.

PATIENT SAFTY

Urge patient to read and follow printed information that explains how to use cabergoline for best therapeutic results.

Advise patient to take drug with meals to help decrease GI distress.

Tell patient to take a missed dose as soon as possible within 1 to 2 days. If missed dose isn’t remembered until it’s time for the next dose, instruct him to double the cabergoline 164 dose if drug is generally well tolerated and doesn’t cause nausea. If drug isn’t well tolerated, instruct patient to consult prescriber before taking the missed dose.

Urge patient to change positions slowly to avoid orthostatic hypotension. Tell him to notify prescriber if it occurs.

Urge patient to keep regular appointments to monitor drug effectiveness.

Advise patient that drug therapy will end when serum prolactin level is normal for 6 months. Explain that he’ll need periodic monitoring to determine whether therapy should resume.

Tell female patient to notify prescriber if she is, could be, or plans to become pregnant during therapy; drug may need to be discontinued.

Caution patient to avoid gambling during therapy because drug may increase the risk of pathological gambling behaviors.

Category

Chemical class: Sterol derivative, vitamin D analogue
Therapeutic class: Antihypocalcemic

Pregnancy category: C

Indications

To treat metabolic bone disease or hypocalcemia in patients receiving renal dialysis Adults and children age 10 and over. 300 to 350 mcg/wk given in divided doses daily or every other day. Increased at 4-wk intervals, p.r.n. Usual dosage 50 to 100 mcg daily or 100 to 200 mcg every other day. Children ages 2 to 10. 0.05 mg daily. Children up to age 2. 0.02 to 0.05 mg daily.
DOSAGE ADJUSTMENT Dosage decreased to as low as 20 mcg every other day in patients with normal serum calcium level. Route Onset Peak Duration P.O. Unknown Unknown 15–20 days

Mechanism of Action

Is converted to calcitriol in kidneys and then binds to specific receptors in intestinal mucosa to increase calcium absorption from intestine. Calcifediol also may regulate calcium ion transfer from bone to blood and stimulate calcium reabsorption in distal renal tubules, making more calcium available in the body.

Contraindications

Abnormal sensitivity to vitamin D effects, decreased renal function, hypercalcemia, hyperphosphatemia, hypervitaminosis, malabsorption syndrome, vitamin D toxicity

Interactions

aluminum-containing antacids: Increased blood aluminum level, especially in patients with chronic renal failure barbiturates, corticosteroids, hydantoin anticonvulsants, primidone: Decreased effects of vitamin D calcitonin, etidronate, gallium nitrate, pamidronate, plicamycin: Decreased effects of these calcium (high doses), thiazide diuretics: Increased risk of hypercalcemia cholestyramine, colestipol, mineral oil: Decreased vitamin D absorption digitalis glycosides: Increased risk of arrhythmias from hypercalcemia magnesium-containing antacids: Hypermagnesemia, especially in chronic renal failure phosphorous-containing : Increased risk of hyperphosphatemia verapamil: Increased risk of atrial fibrillation vitamin D derivatives, such as calcitriol, dihydrotachysterol, ergocalciferol: Increased risk of vitamin D toxicity

Cautions

Use calcifediol cautiously in patients with sarcoidosis or other granulomatous disease because of increased sensitivity to effects of vitamin D.

If hypercalcemia develops, expect to stop drug. Calcium level usually returns to normal in 2 to 4 weeks. To manage acute hypercalcemia, give I.V. normal saline solution and possibly a loop diuretic, as prescribed, to enhance diuresis or prepare for dialysis with a calcium-free dialysate if needed. Chronic hypercalcemia may lead to diffuse vascular calcification, nephrocalcalcifediol 165 C cinosis, and other soft-tissue calcification.

If patient receives high-dose or long-term calcifediol therapy, be alert for vitamin D toxicity. Early evidence includes bone pain, constipation, dry mouth, headache, metallic taste, myalgia, nausea, somnolence, vomiting, and weakness. Late evidence includes albuminuria, anorexia, arrhythmias, azotemia, conjunctivitis (calcific), decreased libido, elevated AST and ALT levels, elevated BUN level, generalized vascular calcification, hypercholeterolemia, hypertension, hyperthermia, irritability, mild acidosis, nephrocalcinosis, nocturia, pancreatitis, photophobia, polydipsia, polyuria, pruritus, rhinorrhea, and weight loss.

PATIENT SAFTY

Instruct patient to swallow capsule whole and not to crush or chew it.

Advise patient to consult prescriber before taking OTC .

Instruct patient to store drug tightly capped in a cool, dry place away from direct light.

Encourage patient to eat a balanced diet that includes high in vitamin D and calcium. Calcifediol is most effective with a high-calcium diet.

If patient takes vitamin supplements, warn him not to exceed recommended amounts.

Tell patient to avoid calcium-, phosphate-, and magnesium-containing laxatives and antacids; mineral oil; and vitamin D preparations because they may increase the risk of calcifediol’s toxic effects.

Advise patient to immediately report possible toxicity, such as headache, irritability, nausea, photophobia, vomiting, weakness, and weight loss.

Stress need for follow-up care, including laboratory tests to evaluate progress and identify signs of toxicity early.

Category

Chemical class: Polypeptide hormone
Therapeutic class: Antihypercalcemic, bone resorption inhibitor, osteoporosis therapy adjunct

Pregnancy category: C

Indications

To treat hypercalcemic emergency I.M.OR SUBCUTANEOUS INJECTION
Adults. Initial: 4 international units/kg every 12 hr. Increased after 1 or 2 days, if needed, to 8 international units/kg every 12 hr. Maximum: 8 international units/kg every 6 hr. To treat postmenopausal osteoporosis I.M.OR SUBCUTANEOUS INJECTION(CALCITONIN, SALMON)
Adults.Initial: 100 international units daily, every other day, or 3 times weekly. Maximum: 100 international units daily.
NASAL SPRAY
Adults. 200 international units (1 spray) daily, alternating nostrils. To treat Paget’s disease of the bone I.M.OR SUBCUTANEOUS INJECTION(CALCITONIN, SALMON)
Adults.Initial: 100 international units daily. Maintenance: 50 to 100 international units daily or every other day. Maximum: 100 international units daily. SUBCUTANEOUS INJECTION(CALCITONIN, HUMAN)
Adults.0.5 mg daily, 0.5 mg 2 or 3 times/ wk, or 0.25 mg daily. Route Onset Peak Duration I.M., SubQ In 15 min* 2 hr 6–8 hr

Mechanism of Action

Directly inhibits bone resorption. Besides reducing the serum calcium level, this action slows bone metabolism (a major factor in the development of Paget’s disease) and calcium loss from the bone (a major factor in the development of osteoporosis).

Contraindications

Hypersensitivity to calcitonin, human; calcitonin, salmon; or their components

Interactions

lithium: Possibly decreased lithium level calcitonin 166 * For hypercalcemia; 6 to 24 mo for Paget’s disease. For hypercalcemia; unknown for other indications.

Side Efect

CNS: Agitation, anxiety, dizziness, headache, insomnia, neuralgia, paresthesia, stroke, vertigo
CV: Bundle-branch block, hypertension, MI, palpitations, peripheral edema, tachycardia, thrombophlebitis
EENT: Blurred vision; dry mouth; earache; epistaxis; eye pain; hearing loss; nasal irritation, lesions, or redness; pharyngitis; rhinitis; salty taste; sinusitis; taste perversion; tinnitus; vitreous floaters
ENDO: Goiter, hyperthyroidism
GI: Abdominal pain, anorexia, cholelithiasis, diarrhea, epigastric discomfort, flatulence, gastritis, hepatitis, increased appetite, nausea, thirst, vomiting
GU: Hematuria, nocturia, pyelonephritis, renal calculi
HEME: Anemia
MS: Arthritis, arthrosis, back pain, joint stiffness, polymyalgia rheumatica
RESP: Bronchitis, bronchospasm, cough, dyspnea, pneumonia, upper respiratory tract infection
SKIN: Alopecia, diaphoresis, eczema, flushing of face or hands, pruritus of earlobes, rash, ulceration
Other: Anaphylaxis, anaphylactic shock, angioedema, antibody formation, feverish sensation, injection site inflammation, lymphadenopathy, mild tetanic symptoms

Cautions

If sensitivity to calcitonin, human; calcitonin, salmon; or their components is suspected, expect to perform a skin test before giving drug. Prepare a mixture of 10 international units/ml by withdrawing 0.05 ml from a 200–international units solution in a tuberculin syringe and filling the syringe to 1 ml with sodium chloride for injection. Mix well, discard 0.9 ml, and inject 0.1 ml intradermally on the inner forearm. Observe the site for 15 minutes after injection. If you detect evidence of sensitivity, such as more than mild erythema or a wheal, notify prescriber.

If patient receives calcitonin for hypercalcemia, monitor serum calcium level. During first several doses, keep parenteral calcium available in case the calcium level is inadvertently overcorrected.

If prescribed calcitonin dose exceeds 2 ml, expect to use I.M. route and multiple injection sites.

For patient receiving calcitonin for postmenopausal osteoporosis, also expect to give 1.5 g supplemental calcium carbonate and at least 400 units vitamin D daily. Plan to provide a balanced diet that includes high in calcium and vitamin D.

Assess for nausea, especially with the first dose. Nausea tends to decrease or disappear with continued use.

If patient with Paget’s disease relapses after treatment, check for antibody formation, as ordered.

PATIENT SAFTY

Tell patient to refrigerate injection or unopened
NASAL SPRAY container.

Teach patient to self-administer injections.

If patient has postmenopausal osteoporosis, teach her about dietary needs, including rich in calcium and vitamin D.

For
NASAL SPRAY, explain how to activate nasal pump by holding the bottle upright and depressing two white side arms toward the bottle six times. When bottle emits a faint spray, pump is activated. Tell patient to store activated nasal pump upright at room temperature and to discard it after 30 days.

Instruct patient to place nozzle firmly into one nostril while holding head upright. Tell him to then depress the pump toward the bottle.

Remind patient that he doesn’t need to reactivate the pump before each dose.

Instruct patient to report nasal symptoms, such as redness, lesions, sinusitis, and rhinitis, to prescriber.

Category

Chemical class: Sterol derivative, vitamin D analogue
Therapeutic class: Antihypocalcemic, antihypoparathyroid

Pregnancy category: C

Indications

To treat hypocalcemia in dialysis patients calcitriol 167 C ,
Adults. Initial: 0.25 mcg daily. Increased by 0.25 mcg daily every 4 to 8 wk, if needed to achieve normal serum calcium level. Maintenance: 0.5 to 3 mcg daily. To treat hypocalcemia in predialysis patients , Adults and children age 3 and over. Initial: 0.25 mcg daily. Increased after 4 to 8 wk, if needed, to 0.5 mcg daily.

ORALL

Children up to age 3. 10 to 15 ng/kg daily. To treat hypoparathyroidism Adults and children age 6 and over. Initial: 0.25 mcg daily in the morning. Increased every 2 to 4 wk, if needed to achieve normal serum calcium level. Usual: 0.5 to 2 mcg daily. Children ages 1 to 5. 0.25 to 0.75 mcg daily in the morning.
I.V.INJECTION
Adults. Initial: 1 to 2 mcg 3 times/wk given every other day. Each dose increased 0.5 to 1 mcg at 2to 4-wk intervals, if needed. Route Onset Peak Duration P.O. 2–6 hr 10 hr 3–5 days

Mechanism of Action

Binds to specific receptors on intestinal mucosa to increase calcium absorption from intestine. Drug also may regulate calcium ion transfer from bone to blood and stimulate calcium reabsorption in the distal renal tubules, making more calcium available in the body.

Contraindications

Hypercalcemia, vitamin D toxicity

Interactions

cholestyramine: Decreased calcitriol absorption digitalis glycosides: Possibly arrhythmias
ketoconazole: Decreased calcitriol level magnesium-containing antacids (I.V. form): Hypermagnesemia mineral oil: Decreased blood calcitriol level (with prolonged use of mineral oil) phenobarbital,
phenytoin: Decreased synthesis and blood level of calcitriol thiazide diuretics: Hypercalcemia

Side Efect

SKIN: Erythema multiforme, lip swelling, pruritus, rash, urticaria
Other: Anaphylaxis

Cautions

Make sure patient receives enough calcium.

Store drug at room temperature, and protect from heat and direct light.

In high-dose or long-term calcitriol therapy, be alert for vitamin D toxicity. Early evidence includes abdominal or bone pain, constipation, dry mouth, headache, metallic taste, myalgia, nausea, somnolence, vomiting, and weakness. Late evidence includes albuminuria, anorexia, arrhythmias, azotemia, conjunctivitis (calcific), decreased libido, elevated AST and ALT levels, elevated BUN level, vascular calcification, hypercholesterolemia, hypertension, hyperthermia, irritability, mild acidosis, nephrocalcinosis, nocturia, pancreatitis, photophobia, polydipsia, polyuria, pruritus, rhinorrhea, and weight loss.

PATIENT SAFTY

Warn patient not to take other forms of vitamin D while taking calcitriol.

Instruct patient to take a missed dose as soon as possible.

Advise patient to notify prescriber immediately about possible toxicity, such as headache, irritability, nausea, photophobia, vomiting, weakness, and weight loss.

Category

Chemical class: Elemental cation
Therapeutic class: Antacid, antihypermagnesemic, antihyperphosphatemic, antihypocalcemic, calcium replacement, cardiotonic

Pregnancy category: C

(Not rated for calcium carbonate, citrate, and lactate)

Indications

To treat hyperphosphatemia (CALCIUM ACETATE)
Adults. Initial: 2 tablets (338 mg elemental calcium, 1,334 mg calcium acetate) t.i.d. with meals. Dosage increased to reduce serum phosphorus level below 6 mg/dl as long as hypercalcemia doesn’t develop. Maintenance: 3 or 4 tablets t.i.d. with each meal. To prevent hypocalcemia , ORAL SUSPENSION,(CALCIUM CARBONATE); EFFERVESCENT , (CALCIUM CITRATE); SYRUP(CALCIUM GLUBIONATE); (CALCIUM GLUCONATE OR LACTATE) Adults and children over age 10. 800 to 1,200 mg daily. Pregnant and breast-feeding women. 1,200 mg daily. Children ages 4 to 10. 800 mg daily. Children up to age 4. 400 to 800 mg daily. To provide antacid effects CHEWABLE , ORAL SUSPENSION, (CALCIUM CARBONATE) Adults and children age 12 and over. 350 to 1,500 mg 1 hr after meals and at bedtime, p.r.n. To replace calcium in hypocalcemia
IV:(CALCIUM CHLORIDE)
Adults.0.5 to 1 g every 1 to 3 days, infused at less than 1 ml/min. Children.25 mg/kg given over several minutes. I.V.OR
I.M.INJECTION(CALCIUM GLUCEPTATE) Adults and children.0.44 to 1.1 g I.M. or 1.1 to 4.4 g I.V. at a rate of no more than 2 ml (36 mg)/min.
I.V.INJECTION(CALCIUM GLUCONATE)
Adults.970 mg given slowly, repeated if needed, until tetany is controlled. Children. 200 to 500 mg as a single dose given slowly, repeated if needed, until tetany is controlled. As adjunct to treat magnesium intoxication
I.V.INJECTION(CALCIUM CHLORIDE)
Adults.500 mg promptly and repeated p.r.n., based on response. As adjunct in cardiac resuscitation
I.V.INJECTION(CALCIUM CHLORIDE)
Adults. 0.5 to 1 g. Children.0.2 ml/kg. As adjunct in exchange transfusion
I.V.INJECTION(CALCIUM GLUCONATE)
Adults.1.35 mEq with each 100 ml of citrated blood exchanged. Neonates. 0.45 mEq after each 100 ml of citrated blood exchanged.
I.V.INJECTION(CALCIUM GLUCEPTATE) Neonates.110 mg after each 100 ml of citrated blood exchanged.

Mechanism of Action

Increases levels of intracellular and extracellular calcium, which is needed to maintain homeostasis, especially in the nervous and musculoskeletal systems. Also plays a role in normal cardiac and renal function, respiration, coagulation, and cell membrane and capillary permeability. Helps regulate the release and storage of neurotransmitters and hormones. Oral forms also neutralize or buffer stomach acid to relieve discomfort caused by hyperacidity.

Contraindications

Hypercalcemia, hypersensitivity to calcium salts or their components, hypophosphatemia, renal calculi

Incompatibilities

To avoid precipitation, don’t give I.V. calcium chloride, gluceptate, or gluconate through same I.V. line as bicarbonates, carbonates, phosphates, sulfates, or tartrates.

Interactions

aluminum-containing antacids: Enhanced aluminum absorption with use of calcium citrate atenolol: Decreased blood atenolol level and calcium 169 C beta blockade calcitonin: Possibly antagonized effects of calcitonin in hypercalcemia treatment calcium supplements, magnesium-containing preparations: Increased serum calcium or magnesium level, especially in patients with impaired renal function cellulose sodium phosphate: Decreased effectiveness of cellulose sodium phosphate in preventing hypercalciuria digitalis glycosides: Increased risk of arrhythmias estrogens, oral contraceptives (estrogen-containing): Increased calcium absorption etidronate: Decreased etidronate absorption fluoroquinolones: Reduced fluoroquinolone absorption by calcium carbonate gallium nitrate: Antagonized effects of gallium nitrate iron salts: Decreased gastric iron absorption magnesium sulfate (parenteral): Neutralized effects of magnesium by parenteral calcium neuromuscular blockers (except succinylcholine): Possibly reversal of neuromuscular blockade by parenteral calcium salts; enhanced or prolonged neuromuscular blockade induced by tubocurarine norfloxacin: Decreased norfloxacin bioavailability
phenytoin: Decreased bioavailability of phenytoin and calcium potassium phosphates, potassium and sodium phosphates: Increased risk of calcium deposition in soft tissue sodium bicarbonate: Possibly milk-alkali syndrome sodium fluoride: Reduced fluoride and calcium absorption sodium polystyrene sulfonate: Possibly metabolic alkalosis if patient has renal impairment tetracyclines: Decreased tetracycline absorption and blood level, leading to decreased anti-infective response thiazide diuretics: Possibly hypercalcemia verapamil: Reversed verapamil effects vitamin A (more than 25,000 units daily): Possibly stimulation of bone loss, decreased effects of calcium supplementation, and hypercalcemia vitamin D (high doses): Excessively increased calcium absorption caffeine, high-fiber food: Possibly decreased calcium absorption alcohol use (excessive), smoking: Possibly decreased calcium absorption

Side Efect

CNS: Paresthesia (parenteral form)
CV: Hypotension, irregular heartbeat (parenteral form)
GI: Nausea or vomiting (parenteral form)
SKIN: Diaphoresis, flushing, or sensation of warmth (parenteral form)
Other: Hypercalcemia; injection site burning, pain, rash, or redness (parenteral form)

Cautions

Store at room temperature, and protect from heat, moisture, and direct light. Don’t freeze.

Warm solution to room temperature before parenteral administration.

Keep patient in a recumbent position for 30 minutes after parenteral administration to prevent dizziness from hypotension.

Administer I.V. calcium through an infusing I.V. solution using a small-bore needle inserted into a large vein to minimize irritation. Give calcium slowly to prevent excess calcium from reaching the heart and causing adverse cardiovascular reactions.

Side Efect

often result from too-rapid administration. If ECG tracings are abnormal or patient reports injection site discomfort, expect to temporarily discontinue administration.

Check regularly for infiltration because calcium causes necrosis. If infiltration occurs, stop infusion and tell prescriber immediately.

Divide I.M. calcium gluceptate dose of 5 ml or more in half and inject in gluteal region.

Regularly monitor serum calcium level and evaluate therapeutic response by assessing for Chvostek’s and Trousseau’s signs, which shouldn’t appear.

Be aware that calcium chloride injection contains three times as much calcium per milliliter as calcium gluconate injection.

PATIENT SAFTY

For chewable tablets, urge patient to chew thoroughly before swallowing and to drink a glass of water afterward.

If suspension is prescribed, tell patient to shake bottle well before each use.

If calcium citrate effervescent tablets are calcium 170 prescribed, tell patient to dissolve them in water and drink immediately.

Instruct patient to take calcium carbonate tablets 1 to 2 hours after meals, calcium glubionate syrup before meals (diluted in water or fruit juice, if desired, for an infant or a child), and other forms with meals.

Advise storing calcium at room temperature away from heat, moisture, and light. Warn against freezing suspension or syrup.

Instruct patient to avoid taking calcium within 2 hours of another oral drug because of risk of interactions.

Urge patient to ask prescriber before taking OTC because of risk of interactions.

Tell patient to avoid excessive use of tobacco and excessive consumption of alcoholic beverages, caffeine-containing products, and high-fiber because these substances may decrease calcium absorption.

Category

Chemical class: Angiotensin II receptor antagonist
Therapeutic class: Antihypertensive

Pregnancy category: C

(first trimester), D (later trimesters)

Indications

To manage, or as adjunct in managing, hypertension
Adults. Initial: 16 mg daily. Maintenance: 8 to 32 mg daily or 4 to 16 mg every 12 hr. Maximum: 32 mg daily.
DOSAGE ADJUSTMENT Initial dosage decreased to 2 mg for patients with moderate to severe hepatic impairment and to 4 mg for those with renal impairment, need for hemodialysis, or possibly a risk of hypotension. To treat heart failure in patients with an ejection fraction of 40% or less and NYHA class II–IV to reduce the risk of death from cardiovascular causes and reduce hospitalizations for heart failure
Adults.Initial: 4 mg daily for 2 wk; then doubled every 2 wk as tolerated until reaching target dose of 32 mg daily. Route Onset Peak Duration P.O. In 2 wk 4–5 wk Unknown

Mechanism of Action

Selectively blocks binding of angiotensin (AT) II to AT1receptor sites in many tissues, including vascular smooth muscle and adrenal glands. This inhibits vasoconstrictive and aldosterone-secreting effects of AT II, which reduces blood pressure.

Contraindications

Hypersensitivity to candesartan or its components

Interactions

diuretics, other antihypertensives: Possibly increased risk of hypotension heparin, potassium-sparing diuretics, potassium supplements, potassium-containing salt substitutes: Possibly increased risk of hyperkalemia lithium: Increased blood lithium level

Side Efect

CNS: Dizziness, headache
CV: Hypotension
EENT: Pharyngitis, rhinitis
GI: Elevated liver function test results, hepatitis
GU: Elevated BUN and serum creatinine levels
HEME: Agranulocytosis, leukopenia, neutropenia
MS: Back pain, rhabdomyolysis
RESP: Upper respiratory tract infection
Other: Hyperkalemia, hyponatremia

Cautions

If patient has known or suspected hypovolemia, expect to provide treatment, such as I.V. normal saline solution, as prescribed, to correct it before starting candesartan.

Monitor patient closely during major surgery and anesthesia because candesartan increases risk of hypotension by blocking renin-angiotensin system.

Watch for elevated BUN and serum creatinine levels, especially if patient has heart failure or impaired renal function; drug may cause acute renal failure. Report sigcandesartan cilexetil 171 C nificant or persistent increases immediately.

If blood pressure isn’t controlled with candesartan alone, expect to give a diuretic, such as hydrochlorothiazide, as prescribed.
WARNING If patient receives a diuretic or antihypertensive with candesartan, has heart failure, or is elderly, assess blood pressure often because of added risk of hypotension.

If patient develops hypotension, expect to stop drug temporarily. Immediately place patient in supine position and prepare to give I.V. normal saline solution, as prescribed. Expect to resume therapy after blood pressure stabilizes.

If patient receives a diuretic, provide hydration, as ordered, to help prevent hypovolemia. Watch for evidence, such as hypotension with dizziness and fainting. If patient has heart failure and develops hypotension, dosage of diuretic, candesartan, or both may be reduced when blood pressure stablizes and therapy resumes.

Check CBC for decreases in hemoglobin and hematocrit. If they’re significant or persistent, notify prescriber immediately.

PATIENT SAFTY

Advise patient that full effects of candesartan may not occur for 4 to 5 weeks.

Explain importance of lifestyle choices in controlling hypertension.

Advise female patient to immediately report known or suspected pregnancy. Explain that if she becomes pregnant, prescriber may replace candesartan with another antihypertensive that’s safe to use during pregnancy.

Category

Chemical class: Polypeptide antibiotic isolated from Streptomyces capreolus
Therapeutic class: Antitubercular

Pregnancy category: C

Indications

As adjunct to treat pulmonary tuberculosis caused by Mycobacterium tuberculosis in which primary are ineffective or can’t be used because of toxicity
IV:,
I.M.INJECTION
Adults.1 g daily for 60 to 120 days followed by 1 g 2 or 3 times/wk for 12 to 24 mo. Maximum: 20 mg/kg daily.
DOSAGE ADJUSTMENT For patient with renal impairment, dosage reduced according to patient’s creatinine clearance.

Mechanism of Action

May interfere with lipid and nucleic acid biosynthesis in actively growing tubercle bacilli.

Contraindications

Hypersensitivity to capreomycin or its components

Interactions

aminoglycosides (parenteral): Increased risk of ototoxicity, nephrotoxicity, and neuromuscular blockade nephrotoxic , such as amphotericin B: Increased risk of nephrotoxicity nondepolarizing neuromuscular blockers: Enhanced neuromuscular blockade ototoxic , such as
quinidine: Increased risk of ototoxicity polymyxins (parenteral): Increased risk of nephrotoxicity and neuromuscular blockade

Side Efect

CNS: Dizziness, vertigo
EENT: Ototoxicity
GI: Elevated liver function test results
GU: Nephrotoxicity
HEME: Leukocytosis, leukopenia
SKIN: Maculopapular rash, sterile abscess, urticaria
Other: Hypocalcemia, hypokalemia, hypomagnesemia, injection site pain, induration, and bleeding

Cautions

Use capreomycin cautiously in patients with renal insufficiency, impaired hearing, or a history of hypersensitivity, especially to other .

Expect to obtain baseline renal function studies, as ordered, before starting capreomycin and weekly throughout therapy because drug may alter renal function.

To reconstitute drug for I.V. injection, add 100 ml normal saline solution. Administer over 60 minutes.

To reconstitute drug for I.M. injection, add 2 ml sodium chloride for injection or capreomycin sulfate 172 sterile water for injection to each 1-g vial. Allow 2 to 3 minutes for complete dissolution.

Give I.M. injection deep into a large muscle mass, such as the gluteus maximus.

Observe injection site for excessive bleeding or sterile abscess.

Make sure patient receives regular audiometric and vestibular function assessment.

Closely monitor patient for urticaria and maculopapular rash.

Check serum electrolyte levels periodically, as ordered, because capreomycin may cause imbalances such as hypocalcemia, hypokalemia, and hypomagnesemia.

PATIENT SAFTY

Advise patient to alert nurse or prescriber if injection site bleeds excessively.

Warn patient to contact prescriber immediately about hearing loss or tinnitus.

Explain the need for frequent laboratory tests to monitor renal function.

Tell patient that tuberculosis therapy lasts for 12 to 24 months.

Explain that noncompliance may decrease effectiveness and lengthen treatment.

Category

Chemical class: ACE inhibitor
Therapeutic class: Antihypertensive

Pregnancy category: C

(first trimester), D (later trimesters)

Indications

To control hypertension Adults and adolescents. Initial: 25 mg b.i.d. or t.i.d. Increased to 50 mg b.i.d. or t.i.d. after 1 to 2 wk, if needed. If blood pressure isn’t well controlled at this dosage and with the addition of a diuretic, dosage increased to 100 mg b.i.d. or t.i.d. and then, if needed, to 150 mg b.i.d. or t.i.d. while continuing diuretic. Maximum: 450 mg daily. To control accelerated or malignant hypertension when temporary discontinuation of current antihypertensive therapy isn’t practical or when prompt titration of blood pressure is needed Adults and adolescents. Initial: 25 mg b.i.d. or t.i.d while continuing diuretic but discontinuing current antihypertensive drug. Increased every 24 hr as needed until satisfactory response is obtained or maximum dosage is reached. Maximum: 450 mg daily. To treat heart failure that’s unresponsive to conventional therapy Adults and adolescents. Initial: 25 mg b.i.d. or t.i.d. Increased to 50 mg b.i.d. or t.i.d., as needed. After 14 days, increased to 100 mg t.i.d. and then to 150 mg t.i.d, if needed. Maximum: 450 mg daily. To treat left-sided heart failure after MI Adults and adolescents.Initial: 6.25 mg as single dose starting 3 days after MI and then 12.5 mg t.i.d. Increased to 25 mg t.i.d. for several days and then again to maintenance dosage. Maintenance: 50 mg t.i.d. To treat diabetic nephropathy Adults and adolescents. 25 mg t.i.d.
DOSAGE ADJUSTMENT Starting dosage reduced to 6.25 mg b.i.d. or t.i.d. if patient with hypertension also has heart failure, is undergoing dialysis, or is being vigorously treated with diuretics that result in hyponatremia or hypovolemia. Route Onset Peak Duration P.O. 15–60 min 60–90 min 6–12 hr

Mechanism of Action

By inhibiting angiotensin-converting enzyme, captopril:

prevents conversion of angiotensin I to angiotensin II, a potent vasoconstrictor that also stimulates the adrenal cortex to secrete aldosterone. Inhibiting aldosterone increases sodium and water excretion, reducing blood pressure.

may inhibit renal and vascular production of angiotensin II.

decreases serum angiotensin II level and increases renin activity. This decreases aldosterone secretion, slightly increasing serum potassium level and fluid loss.

decreases vascular tone and blood pressure.

Contraindications

Hypersensitivity to captopril, other ACE inhibitors, or their components captopril 173 C

Interactions

allopurinol: Increased risk of hypersensitivity reactions, including Stevens-Johnson syndrome, skin eruptions, fever, arthralgia antacids: Possibly impaired captopril absorption capsaicin: Possibly cause or worsening of cough from ACE inhibitor cyclosporine, potassium-containing , potassium-sparing diuretics, potassium supplements: Increased risk of hyperkalemia digoxin: Increased blood digoxin level diuretics; hypotension-producing , such as hydralazine: Additive hypotensive effects gold: Increased risk of nitritoid reaction, including facial flushing, nausea, vomiting, and hypotension lithium: Increased risk of lithium toxicity
NSAIDs: Decreased antihypertensive response to ACE inhibition probenecid: Increased blood level and decreased total clearance of captopril
alcohol use: Additive hypotensive effects

Side Efect

CNS: Fever
CV: Chest pain, hypotension, orthostatic hypotension, palpitations, tachycardia
EENT: Loss of taste
GU: Dysuria, impotence, nephrotic syndrome, nocturia, oliguria, polyuria, proteinuria, urinary frequency
HEME: Eosinophilia
MS: Arthralgia
RESP: Cough
SKIN: Photosensitivity, pruritus, rash
Other: Angioedema, hyperkalemia, hyponatremia, positive ANA titer

Cautions

Closely monitor patient’s blood pressure, especially when therapy starts and dosage increases. Keep patient supine if hypotension occurs.

Monitor renal function tests for signs of nephrotic syndrome, such as proteinuria and increased BUN and serum creatinine levels. Also watch for such renal evidence as oliguria, polyuria, and urinary frequency.

Monitor WBC regularly, as ordered, especially if patient has collagen vascular disease or renal disease.

PATIENT SAFTY

Instruct patient to take captopril 1 hour before meals.

Tell patient to rise slowly from sitting or lying to minimize orthostatic hypotension.

Tell patient to avoid sunlight or wear sunscreen in direct sunlight because photosensitivity may occur.

Warn patient not to stop drug abruptly.

Urge patient not to use salt substitutes that contain potassium and to consult prescriber before increasing potassium intake to avoid increasing risk of hyperkalemia.

Urge patient to tell prescriber about signs and symptoms of infection, such as sore throat or fever.

Category

Chemical class: Tricyclic iminostilbene derivative
Therapeutic class: Analgesic, anticonvulsant

Pregnancy category: C

Indications

To treat epilepsy (CARBATROL), (TEGRETOL-XR) Adults and children age 12 and over. Initial: 200 mg b.i.d. Increased weekly by 200 mg daily, if needed. Maximum: 1,600 mg daily in adults, 1,200 mg daily in children age 16 and over, and 1,000 mg daily in children ages 12 to 16. Children ages 6 to 12. Initial: 100 mg b.i.d. Increased weekly by 100 mg daily, if needed. Maximum: 1,000 mg daily. ORAL SUSPENSION Adults and children age 12 and over. Initial: 100 mg q.i.d. Increased weekly by 200 mg daily, if needed, given in divided doses t.i.d or q.i.d. Maximum: 1,600 mg daily in adults, 1,200 mg daily in children age 16 and over, and 1,000 mg daily in children ages 12 to 16. Children ages 6 to 12. Initial: 50 mg q.i.d. Increased weekly by 100 mg daily, if needed, given in divided doses t.i.d or q.i.d. Maximum: 1,000 mg daily. Children up to age 6. Initial: 10 to 20 mg/ carbamazepine 174 kg/day in divided doses q.i.d. Maximum: 35 mg/kg daily. Adults and children age 12 and over. Initial: 200 mg b.i.d. Increased weekly by 200 mg/day, if needed, given in divided doses t.i.d. or q.i.d. Maximum: 1,600 mg daily in adults, 1,200 mg daily in children age 16 and over, and 1,000 mg daily in children ages 12 to 16. Children ages 6 to 12. Initial: 100 mg b.i.d. Increased weekly by 100 mg daily, if needed, given in divided doses t.i.d. or q.i.d. Maximum: 1,000 mg daily. Children up to age 6. Initial: 10 to 20 mg/ kg daily in divided doses b.i.d. or t.i.d. Increased weekly, if needed, divided and given t.i.d. or q.i.d. Maximum: 35 mg/kg/day. To relieve pain in trigeminal neuralgia (CARBATROL), (TEGRETOL-XR),
Adults.Initial: 100 mg b.i.d. Increased by up to 200 mg daily, if needed, in increments of 100 mg every 12 hr. Maintenance: 400 to 800 mg/day. Maximum: 1,200 mg daily. ORAL SUSPENSION(100 MG/5 ML)
Adults.50 mg q.i.d. Increased by up to 200 mg daily, if needed, in increments of 50 mg q.i.d. Maintenance: 400 to 800 mg daily. Maximum: 1,200 mg daily. To treat acute manic and mixed episodes in bipolar disorder (EQUETRO)
Adults. Initial: 200 mg b.i.d., increased as needed in 200-mg increments. Maximum: 1,600 mg daily.

Contraindications

History of bone marrow depression; hypersensitivity to carbamazepine, tricyclic compounds, or their components; MAO inhibitor or nefazodone therapy Route Onset Peak Duration P.O. (all In 1 mo* Unknown Unknown forms)

Interactions

acetaminophen (long-term use): Increased metabolism, leading to acetaminopheninduced hepatotoxicity or decreased acetaminophen effectiveness acetazolamide, cimetidine, clarithromycin, danazol, diltiazem, erythromycin, fluconazole, fluoxetine, fluvoxamine, isoniazid, itraconazole, ketoconazole, loratadine, niacinamide, nicotinamide, propoxyphene, protease inhibitors, terfenadine, troleandomycin, valproate, verapamil: Increased blood carbamazepine level alprazolam, amitriptyline, bupropion, buspirone, citalopram, clobazam, clonazepam, clozapine, cyclosporine, delavirdine, desipramine, diazepam, dicumarol, doxycycline, ethosuximide, felodipine, glucocorticoids, haloperidol, itraconazole, lamotrigine, levothyroxine, lorazepam, methadone, methsuximide, midazolam, mirtazapine, nortriptyline, olanzapine, oral contraceptives, oxcarbazepine, phenytoin, praziquantel, protease inhibitors, quetiapine, risperidone, theophylline, tiagabine, topiramate, tramadol, triazolam, trazodone, valproate, warfarin, carbamazepine 175 C

Mechanism of Action

Normally, sodium moves into a neuronal cell by passing through a gated sodium channel in the cell membrane. Carbamazepine may prevent or halt seizures by closing or blocking sodium channels, as shown below, thus preventing sodium from entering the cell. Keeping sodium out of the cell may slow nerve impulse transmission, thus slowing the rate at which neurons fire. * For anticonvulsant use; 8 to 72 hr for use in trigeminal neuralgia. Cell exterior Sodium Open sodium channel Closed sodium channel Carbamazepine Neuronal cell membrane Cell interior ziprasidone, zonisamide: Decreased blood levels of these cisplatin, doxorubicin, felbamate, methsuximide, phenytoin, rifampin,
theophylline: Decreased blood carbamazepine level clomipramine, phenytoin, primidone: Increased blood levels of these felbamate: Decreased blood level of felbamate or carbamazepine isoniazid: Increased risk of carbamazepine toxicity and isoniazid hepatotoxicity lamotrigine, phenobarbital, primidone, tricyclic antidepressants,
valproic acid: Decreased blood levels of these , increased blood level of carbamazepine lithium: Increased risk of CNS toxicity nefazodone: Decreased nefazodone effectiveness and increased carbamazepine level nondepolarizing neuromuscular blockers: Possibly reduced duration or decreased effectiveness of neuromuscular blocker oral anticoagulants: Increased metabolism and decreased effectiveness of anticoagulant grapefruit juice: Increased blood carbamazepine level
alcohol use: Increased sedative effect

Side Efect

CNS: Chills, confusion, dizziness, drowsiness, fatigue, fever, headache, suicidal ideation, syncope, talkativeness, unsteadiness, visual hallucinations
CV: Arrhythmias, including AV block; edema; heart failure; hypertension; hypotension; thromboembolism; thrombophlebitis; worsened coronary artery disease
EENT: Blurred vision, conjunctivitis, dry mouth, glossitis, nystagmus, oculomotor disturbances, stomatitis, tinnitus, transient diplopia
ENDO: Syndrome of inappropriate ADH secretion, water intoxication
GI: Abdominal pain, anorexia, constipation, diarrhea, dyspepsia, elevated liver function test results, hepatitis, nausea, pancreatitis, vomiting
GU: Acute urine retention, albuminuria, azotemia, glycosuria, impotence, oliguria, renal failure, urinary frequency HEME:Acute intermittent porphyria, agranulocytosis, aplastic anemia, bone marrow depression, eosinophilia, leukocytosis, leukopenia, pancytopenia, thrombocytopenia
MS: Arthralgia, leg cramps, myalgia
RESP: Pulmonary hypersensitivity (dyspnea, fever, pneumonia, or pneumonitis)
SKIN: Aggravation of disseminated lupus erythematosus, alopecia, altered skin pigmentation, diaphoresis, erythema multiforme, erythema nodosum, exfoliative dermatitis, jaundice, Lyell’s syndrome, photosensitivity reactions, pruritic and erythematous rash, purpura, Stevens-Johnson syndrome, urticaria
Other: Adenopathy, lymphadenopathy

Cautions

Avoid using carbamazepine in patients with a history of hepatic porphyria because it may prompt an acute attack.
WARNING If patient has Asian ancestry, make sure he has been evaluated for the genetic allelic variant HLA-B 1502 before starting carbamazepine therapy. Patients positive for HLA-B 1502 shouldn’t take carbamazepine because the risk of serious, sometimes fatal, dermatologic reactions is ten times higher than in patients without this variant.

Use carbamazepine cautiously in patients with impaired hepatic function because it’s mainly metabolized in the liver. Monitor liver function tests, as directed.

Monitor patient closely for adverse reactions because many are serious.

Periodically monitor blood carbamazepine level to assess for therapeutic and toxic levels; a blood level of 6 to 12 mcg/ml is optimal for anticonvulsant effects.
WARNING Monitor WBC and platelet counts monthly for first 2 months. Decreased counts may indicate bone marrow depression.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

Withdraw carbamazepine gradually to minimize risk of seizures.

PATIENT SAFTY

Tell patient to take carbamazepine with food (except the oral suspension form, which shouldn’t be taken with other liquid or diluents).

Warn patient about possible dizziness, blurred vision, and unsteadiness.

Inform patient that coating of tablets isn’t absorbed and may appear in stool. carbamazepine 176

Advise patient not to crush or chew capsules or tablets. If he can’t swallow capsules whole, have him open them and sprinkle contents on food.

Urge patient to wear sunscreen and protective clothing to reduce photosensitivity.

Tell patient to report unusual bleeding or bruising, fever, rash, or mouth ulcers.

Tell woman that drug decreases oral contraceptive effectiveness, and urge her to use different contraception. Because drug may cause fetal harm, tell her to notify prescriber about possible pregnancy.

If she becomes pregnant during therapy, urge her to enroll in the antiepileptic drug pregnancy registry by calling 1-888-2332334. Explain that the registry is collecting information about the safety of antiepileptic during pregnancy.

Instruct caregivers to watch patient closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes, and to report such tendencies to prescriber immediately.

Category

Chemical class: Dicarbamate
Therapeutic class: Skeletal muscle relaxant

Pregnancy category: C

Indications

As adjunct to relieve acute musculoskeletal pain and stiffness (SOMA) Adults and children over age 16. 250 to 350 mg t.i.d. and at bedtime. (VANADOM) Children ages 5 to 12. 6.25 mg/kg t.i.d. and at bedtime. Route Onset Peak Duration P.O. 30 min Unknown 4–6 hr

Mechanism of Action

Blocks interneuronal activity in descending reticular formation and spinal cord, producing muscle relaxation and sedation.

Contraindications

Hypersensitivity or idiosyncratic reactions to carisoprodol, to its components, or to meprobamate-related compounds; intermittent porphyria

Interactions

CNS depressants, psychotropic : Additive CNS depression fluvoxamine, omeprazole: Increased blood carisoprodol level rifampin,
St. John’s wort: Decreased blood carisoprodol level
alcohol use: Additive CNS depression

Side Efect

CNS: Agitation, ataxia, depression, dizziness, drowsiness, fever, headache, insomnia, irritability, seizures, somnolence, syncope, tremor, vertigo
CV: Orthostatic hypotension, tachycardia
EENT: Diplopia, transient vision loss
GI: Epigastric discomfort, hiccups, nausea, vomiting
HEME: Eosinophilia
SKIN: Erythema multiforme, facial flushing, pruritus, rash
Other: Drug dependence or withdrawal

Cautions

Use carisoprodol cautiously in patients with history of drug addiction and in patients taking other CNS depressants, including alcohol.

Carisoprodol therapy should last no longer than 3 weeks.

Monitor patient closely for hypersensitivity or idiosyncratic reactions. They typically occur before the fourth dose in patients who have no previous carisoprodol exposure.

Provide rest and other pain-relief measures.

To avoid mild withdrawal symptoms, expect to taper therapy as prescribed, rather than stopping it abruptly.

PATIENT SAFTY

Tell patient to take carisoprodol with meals if GI distress occurs.

Caution patient that drug dependence and withdrawal may occur, especially if therapy lasts a long time or patient changes dosage without consulting prescriber.

Warn patient about possible dizziness, drowsiness, syncope, and vertigo. Discourage hazardous activities, such as driving, until effects of drug are known. carisoprodol 177 C

Inform patient that abruptly stopping drug can cause headache, insomnia, nausea, and other

Side Efect

.

Instruct patient to avoid alcohol and other CNS depressants while taking drug.

Explain that saliva, urine, and sweat may appear darker (red, brown, or black). Reassure him that this discoloration is harmless but may stain garments.

Tell patient to store drug in a tightly capped container at room temperature.

Tell patient not to store drug in bathroom, near kitchen sink, or in other damp places to protect it from heat and moisture.

Category

Chemical class: Beta-adrenergic blocker
Therapeutic class: Antihypertensive

Pregnancy category: C

Indications

To control hypertension
Adults. Initial: 2.5 mg daily. If response is inadequate, dosage increased to 5 mg and then 10 mg daily, p.r.n. Maintenance: 2.5 or 5 mg daily.
DOSAGE ADJUSTMENT Interval increased to every 48 hr for patients with creatinine clearance of 20 to 60 ml/min/1.73 m2or to every 72 hr for clearance of less than 20 ml/ min/1.73 m2. Route Onset Peak Duration P.O. Unknown 1–3 hr Unknown

Mechanism of Action

May reduce blood pressure by competing with beta-adrenergic receptor agonists, which helps reduce cardiac output, decrease sympathetic outflow to peripheral blood vessels, and inhibit renin.

Contraindications

Asthma, bradycardia (less than 45 beats/ min), cardiogenic shock, hypersensitivity to carteolol or its components, secondor third-degree heart block

Interactions

allergen immunotherapy, allergenic extracts for skin testing: Increased risk of serious systemic reaction or anaphylaxis catecholamine-depleting , such as reserpine: Additive effects, increased risk of hypotension and bradycardia
clonidine: Increased risk of tachycardia and hypertension after clonidine discontinuation diltiazem, nifedipine, verapamil: Potentiated effects of carteolol general anesthetics: Exaggeration of hypotension
NSAIDs: Reduced antihypertensive effect of carteolol oral antidiabetic : Reduced symptomatic responses to hypoglycemia sympathomimetics with alphaand betaadrenergic effects, such as pseudoephedrine: Possibly hypertension and excessive bradycardia or heart block

Side Efect

CNS: Fatigue, insomnia, lassitude, paresthesia, tiredness, weakness
CV: Chest pain, heart failure, peripheral edema
EENT: Dry mouth, nasal congestion, pharyngitis
GI: Abdominal pain, diarrhea, flatulence, nausea
MS: Arthralgia, back pain, leg pain, muscle spasms
SKIN: Rash

Cautions

WARNING Be aware that stopping carteolol abruptly in patients with angina may cause worsening of angina or MI; abrupt cessation in patients with hyperthyroidism may cause thyroid storm.

Carefully monitor blood glucose level in diabetic patient because carteolol can mask hypoglycemic symptoms. It also can interfere with endogenous insulin release in response to hyperglycemia, requiring adjustment of oral antidiabetic dosage.

PATIENT SAFTY

Advise patient to complete dosing schedule, even if he feels better, and not to discontinue therapy abruptly.

Instruct patient to report signs of heart failure, such as fatigue, difficulty breathcarteolol hydrochloride 178 ing, cough, and unusually fast heartbeat.

Tell diabetic patient to check his blood glucose level often.

Advise patient to consult prescriber before taking OTC preparations, such as nasal decongestants and cold preparations that contain sympathomimetics, because of the risk of serious drug interactions.

Category

Chemical class: Nonselective beta-adrenergic blocker with alpha1-adrenergic blocking activity
Therapeutic class: Antihypertensive, heart failure treatment adjunct

Pregnancy category: C

Indications

To control hypertension
Adults. 6.25 mg b.i.d. for 7 to 14 days, if tolerated. Then dosage increased to 12.5 mg b.i.d. for 7 to 14 days, and up to 25 mg, if tolerated and needed. Maximum: 50 mg daily.
Adults.Initial: 20 mg once daily with food. After 7 to 14 days, increased to 40 mg once daily. After another 7 to 14 days, increased to 80 mg once daily. Maximum: 80 mg once daily. As adjunct to treat mild to severe heart failure of ischemic or cardiomyopathic origin
Adults.3.125 mg b.i.d. for 2 wk; then increased to 6.25, 12.5, and 25 mg b.i.d. at successive 2-wk intervals, as tolerated. Maximum (for patients with mild to moderate heart failure): 50 mg b.i.d. if patient weighs more than 85 kg (187 lb).
Adults.Initial: 10 mg once daily with food for 2 wk. Then increased to 20 mg once daily, as needed. Subsequent dosage increased by 20 mg every 2 wk, as needed. Maximum: 80 mg once daily. To reduce CV mortality after acute phase of MI in patients with left ventricular ejection fraction of 40% or less
Adults. 6.25 mg b.i.d. for 3 to 10 days, if tolerated. Then dosage increased to 12.5 mg b.i.d. for 3 to 10 days and up to 25 mg b.i.d., if needed and tolerated.
Adults.Initial: 10 to 20 mg once daily. After 3 to 10 days, increased to 20 to 40 mg once daily. Increased again as needed every 3 to 10 days until reaching tolerance or target dose of 80 mg once daily. Maximum: 80 mg once daily.
DOSAGE ADJUSTMENT For patient with fluid retention or low blood pressure or heart rate, starting dosage may be decreased to 3.125 mg b.i.d., increase may be slowed, or both for tablet form. For patient with heart rate below 55 beats/min, extended-release dosage decreased as clinical condition indicates. Route Onset Peak Duration P.O. In 30 min 1.5–7 hr Unknown

Mechanism of Action

Reduces cardiac output and tachycardia, causes vasodilation, and decreases peripheral vascular resistance, which reduces blood pressure and cardiac workload. When given for at least 4 weeks, carvedilol reduces plasma renin activity.

Contraindications

Asthma or related bronchospastic conditions; cardiogenic shock; decompensated heart failure that requires I.V. inotropics; history of serious hypersensitivity reactions, such as anaphylaxis, angioedema, or Stevens-Johnson syndrome; hypersensitivity to carvedilol or its components; secondor third-degree AV block, severe bradycardia or hepatic impairment, or sick sinus syndrome unless pacemaker is in place

Interactions

amiodarone; other CYP2C9 , such as fluconazole: Increased risk of bradycardia or heart block beta blockers, digoxin: Increased risk of bradycardia calcium channel blockers (especially diltiazem and verapamil): Abnormal cardiac conduction and, possibly, increased adverse effects of calcium channel blockers carvedilol 179 C catecholamine-depleting (such as reserpine, MAO inhibitors): Additive effects, increased risk of hypotension and bradycardia
cimetidine: Increased blood carvedilol level
clonidine: Risk of tachycardia and hypertension when clonidine is discontinued cyclosporine, digoxin: Increased blood levels of these digoxin: Possibly increased digoxin level oral antidiabetics: Increased risk of hypoglycemia
rifampin: Decreased blood carvedilol level

Side Efect

CNS: Asthenia, depression, dizziness, fatigue, fever, headache, hypesthesia, hypotonia, insomnia, light-headedness, malaise, paresthesia, somnolence, stroke, syncope, vertigo
CV: Angina, AV block, bradycardia, edema, heart failure, hypertension, hypertriglyceridemia, orthostatic hypotension, palpitations, peripheral vascular disorder
EENT: Blurred vision, dry eyes, periodontitis, pharyngitis, rhinitis
ENDO: Hyperglycemia, hypoglycemia
GI: Abdominal pain, diarrhea, elevated liver function test results, melena, nausea, vomiting
GU: Albuminuria, hematuria, elevated BUN and creatinine levels, impotence, renal insufficiency, UTI
HEME: Aplastic anemia, decreased PT, thrombocytopenia, unusual bleeding or bruising
MS: Arthralgia, arthritis, back pain, muscle cramps
RESP: Dyspnea, increased cough
SKIN: Jaundice, pruritus, purpura, urticaria
Other: Anaphylaxis, angioedema, fluid overload, gout, hyperkalemia, hyperuricemia, hyponatremia, hypovolemia, viral infection, weight gain or loss

Cautions

Use carvedilol cautiously in patients with peripheral vascular disease because it may aggravate symptoms of arterial insufficiency. In patients with diabetes mellitus it may mask signs of hypoglycemia, such as tachycardia, and may delay recovery.

Monitor patient’s blood glucose level, as ordered, during carvedilol therapy because drug may alter blood glucose level.
WARNING Avoid stopping drug abruptly in patients with hyperthyroidism because thyroid storm may occur and in patients with angina because it may worsen or MI may occur.

If patient has heart failure, expect to also give digoxin, a diuretic, and an ACE inhibitor. PATIENT TACHING

Instruct patient prescribed extendedrelease capsules to swallow them whole. If swallowing capsules is difficult, tell patient he may open capsule and sprinkle beads on a spoonful of cold applesauce and then eat the applesauce immediately without chewing.

Warn patient that drug may cause orthostatic hypotension, light-headedness, and dizziness; advise him to take precautions.

Tell patient with heart failure to notify prescriber if he gains 5 lb or more in 2 days or if shortness of breath increases, which may signal worsening heart failure.

Alert patient with diabetes to monitor his glycemic control closely because drug may increase blood glucose level or mask symptoms of hypoglycemia.

Stress the need to seek emergency care if patient develops hives or swelling of the face, lips, tongue, or throat that causes trouble swallowing or breathing.

Category

Chemical class: Echinocandins
Therapeutic class: Antifungal

Pregnancy category: C

Indications

To treat invasive aspergillosis in patients refractory to or intolerant of other therapies; to treat candidemia and candidal infections in intra-abdominal abscesses, peritonitis, and pleural space infections

IV

Adults.Initial: 70 mg on day 1, followed by 50 mg daily. Maximum: 70 mg daily. Children ages 3 months to 17 years. Initial: 70 mg/m2on day 1, followed by 50 mg/m2 daily. Maximum: 70 mg daily regardless of caspofungin acetate 180 dose calculated based on patient’s body surface area. To treat presumed fungal infections in febrile, neutropenic patients

IV

Adults.Initial: 70 mg on day 1, followed by 50 mg daily for at least 14 days, including at least 7 days after neutropenia and symptoms have resolved. Increased to 70 mg daily as needed. Maximum: 70 mg daily. Children ages 3 months to 17 years. Initial: 70 mg/m2on day 1, followed by 50 mg/m2 daily for at least 14 days, including at least 7 days after neutropenia and symptoms have resolved. Maximum: 70 mg daily regardless of dose calculated based on patient’s body surface area.
DOSAGE ADJUSTMENT Dosage reduced to 35 mg daily after initial 70-mg loading dose in moderate hepatic insufficiency. To treat esophageal candidiasis

IV

Adults.50 mg daily. Children ages 3 months to 17 years.Initial: 70 mg/m2on day 1, followed by 50 mg/m2 daily. Maximum: 70 mg daily regardless of dose calculated based on patient’s body surface area.
DOSAGE ADJUSTMENT Dosage reduced to 35 mg daily in moderate hepatic insufficiency.

Incompatibilities

Don’t mix or infuse with other . Don’t admix with diluents that contain dextrose.

Contraindications

Hypersensitivity to caspofungin acetate or its components

Interactions

carbamazepine, dexamethasone, efavirenz, nelfinavir, nevirapine, phenytoin,
rifampin: Possibly decreased blood caspofungin level cyclosporine: Transient increases in ALT and AST levels tacrolimus: Possibly decreased blood tacrolimus level

Side Efect

CNS: Chills, dizziness, fever, headache, insomnia, paresthesia, tremor
CV: Edema, hypertension, hypotension, phlebitis, tachycardia, thrombophlebitis
EENT: Mucosal inflammation
GI: Abdominal pain, diarrhea, elevated liver function test results, hepatic dysfunction, jaundice, nausea, vomiting
GU: Elevated BUN or serum creatinine level, proteinuria, renal insufficiency
HEME: Decreased hemoglobin and hematocrit
MS: Back pain, myalgia
RESP: Bronchospasm, cough, crackles, dyspnea, pleural effusion, pneumonia, respiratory failure, stridor, tachypnea
SKIN: Diaphoresis, erythema, flushing, pruritus, rash, sensation of warmth
Other: Anaphylaxis, decreased serum bicarbonate level, facial edema, hypercalcemia, hyperkalemia, hyperphosphatemia, hypokalemia, hypomagnesemia, infusion site reaction, sepsis, septic shock

Cautions

To prepare 70-mg loading dose, let vial caspofungin acetate 181 C Fungal cell exterior Fungal cell interior Inhibited β (1,3)-D-glucan β (1,3)-D-glucan Cell membrane Caspofungin

Mechanism of Action

Caspofungin acetate interferes with fungal cell membrane synthesis by inhibiting the synthesis of b (1,3)-Dglucan. A polypeptide, b (1,3)-Dglucan is the essential component of the fungal cell membrane that makes it rigid and protective. Without it, fungal cells rupture and die. This

Mechanism of Action

is most effective against susceptible filamentous fungi, such as Aspergillus. reach room temperature. Reconstitute by adding 10.5 ml normal saline solution to vial. Dilute for administration by transferring 10 ml of reconstituted drug to 250 ml normal saline solution.

To prepare 70-mg loading dose from two 50-mg vials, add 10.5 ml normal saline solution to each vial; then transfer 14 ml of prepared solution to 250 ml normal saline solution.

To prepare daily 50-mg infusion, let vial reach room temperature. Reconstitute by adding 10.5 ml normal saline solution to vial. Dilute for administration by transferring only 10 ml of reconstituted drug to 250 ml normal saline solution.

To prepare daily 50-mg infusion at reduced volume, add 10 ml of reconstituted drug to 100 ml normal saline solution.

To prepare 35-mg daily dose for patient with moderate hepatic insufficiency, reconstitute 50-mg vial with 10.5 ml normal saline solution. To dilute, transfer only 7 ml of reconstituted drug to 250 ml normal saline solution or, if needed, to 100 ml normal saline solution.

When preparing powder for reconstitution, mix gently to obtain clear solution. Don’t use if solution is cloudy or contains precipitate. Discard unused solution after 24 hours.

Infuse drug slowly over about 1 hour.

Expect to increase daily dose to 70 mg for adults and 70 mg/m2for children (not to exceed the adult dose of 70 mg regardless of calculated dose), as prescribed, for patients also receiving carbamazepine, dexamethasone, efavirenz, nelfinavir, nevirapine, phenytoin, or rifampin.

Watch for flushed skin, and assess patient often for unexplained temperature elevation.

Assess for airway patency if patient develops excessive facial edema or respiratory stridor. Provide emergency airway management if complete obstruction occurs.

Monitor patient’s liver function test results, as ordered, and report abnormalities.

PATIENT SAFTY

Urge patient to notify prescriber immediately if he has difficulty talking, swallowing, or breathing during drug administration.

Category

Chemical class: Second-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat otitis media caused by Haemophilus influenzae, staphylococci, Streptococcus pneumoniae, and Streptococcus pyogenes; lower respiratory tract infections, including pneumonia caused by H. influenzae, S. pneumoniae, and S. pyogenes; pharyngitis and tonsillitis caused by S. pyogenes; UTI, including cystitis and pyelonephritis, caused by Escherichia coli, Klebsiella species, Proteus mirabilis, and coagulase-negative staphylococci; and skin and soft-tissue infections caused by S. pyogenes and Staphylococcus aureus Adults and adolescents. 250 mg every 8 hr. For severe infections, such as pneumonia, or those caused by less susceptible organisms, 500 mg every 8 hr. Maximum: 4 g daily. CHEWABLE , ORAL SUSPENSION Adults and adolescents. 250 mg every 8 hr. For severe infections, such as pneumonia, or those caused by less susceptible organisms, 500 mg every 8 hr. Maximum: 4 g daily. Children. 20 mg/kg daily in divided doses every 8 hr. For serious infections, such as otitis media, and infections caused by less susceptible organisms, 40 mg/kg daily in divided doses every 8 hr. For otitis media and pharyngitis, total daily dosage divided and given every 12 hr, if needed. Maximum: 1 g daily. To treat acute bacterial infection in chronic bronchitis or secondary bacterial infection in acute bronchitis (not caused by H. influenzae) Adults and adolescents age 16 and over. cefaclor 182 500 mg every 12 hr for 7 days. To treat pharyngitis and tonsillitis (not caused by H. influenzae) Adults and adolescents age 16 and over. 375 mg every 12 hr for 10 days. To treat uncomplicated skin and soft-tissue infections caused by S. aureus Adults and adolescents age 16 and over. 375 mg every 12 hr for 7 to 10 days.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting cross-linking of peptidoglycan strands, which stiffen cell membranes. As a result, bacterial cells rupture.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity antacids: Decreased blood cefaclor level ( tablets) oral anticoagulants: Increased anticoagulation

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis, superinfection

Cautions

Use cefaclor cautiously in patients with impaired renal function or a history of GI disease, particularly colitis, and in patients who are hypersensitive to penicillin; about 10% of them have cross-sensitivity.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

Monitor BUN and serum creatinine levels for early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.

Be aware that an allergic reaction may occur a few days after therapy starts.

Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Assess patient for superinfection: perineal itching, fever, malaise, redness, pain, swelling, rash, drainage, diarrhea, cough, sputum changes.

PATIENT SAFTY

Instruct patient to complete the prescribed course of therapy, even if he feels better.

Tell patient to swallow tablets whole and not to crush, break, or chew them.

Advise patient to take tablets with food to enhance absorption.

Instruct patient to take capsules or tablets with a full glass of water.

Tell patient to shake oral suspension well before measuring and to use a calibrated measuring device to ensure accurate dose.

Tell patient to refrigerate oral suspension and to discard unused portion after 14 days.

Instruct patient to immediately report severe diarrhea to prescriber.

Explain that yogurt and buttermilk protect intestinal flora and decrease diarrhea.

Urge patient to report evidence of superinfection.

Category

Chemical class: First-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat UTI caused by Escherichia coli, Klebsiella species, or Proteus mirabilis ,
Adults.For uncomplicated lower UTI, 1 to cefadroxil 183 C 2 g daily or in divided doses every 12 hr. For all other UTIs, 2 g every 12 hr. ORAL SUSPENSION
Adults.For uncomplicated lower UTI, 1 to 2 g daily or in divided doses every 12 hr. For all other UTIs, 2 g every 12 hr. Children.30 mg/kg daily in divided doses every 12 hr. Maximum: Adult dosage. To treat skin and soft-tissue infections caused by staphylococci or streptococci ,
Adults. 1 g daily or 500 mg every 12 hr. ORAL SUSPENSION
Adults. 1 g daily or 500 mg every 12 hr. Children.30 mg/kg daily in divided doses every 12 hr. Maximum: Adult dosage. To treat pharyngitis and tonsillitis caused by group A beta-hemolytic streptococci ,
Adults. 1 g daily or 500 mg b.i.d for 10 days. ORAL SUSPENSION
Adults. 1 g daily or 500 mg b.i.d. for 10 days. Children. 30 mg/kg daily in divided doses every 12 hr for 10 days. Maximum: 1 g daily or 500 mg b.i.d. for 10 days.
DOSAGE ADJUSTMENT Initial dose of 1 g; then maintenance of 0.5 g every 12 hr if creatinine clearance is 25 to 50 ml/min/ 1.73 m2; 0.5 g every 24 hr if creatinine clearance is 10 to 25 ml/min/1.73 m2; and 0.5 g every 36 hr if creatinine clearance is 0 to 10 ml/min/1.73 m2.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased toxicity of these

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis, superinfection

Cautions

Use cefadroxil cautiously in patients with impaired renal function or a history of GI disease, particularly colitis. Also use drug cautiously in patients who are hypersensitive to penicillin because cross-sensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

Be aware that an allergic reaction may occur a few days after therapy starts.

Monitor BUN and serum creatinine levels for early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.

Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Assess for signs of superinfection, such as perineal itching, fever, malaise, redness, pain, swelling, drainage, rash, diarrhea, and cough or sputum changes.

PATIENT SAFTY

Instruct patient to complete the prescribed course of therapy.

Tell patient to shake oral suspension before measuring and to use a liquidmeasuring device to ensure accurate doses.

Tell patient to refrigerate oral suspension and to discard the unused portion after 14 days.

Urge patient to report watery, bloody stools to prescriber immediately, even up to 2 months after drug therapy has ended.

Inform patient that yogurt and buttermilk can help maintain intestinal flora and decrease diarrhea.

Teach patient to recognize and report evidence of superinfection, such as furry tongue, perineal itching, and loose, foulsmelling stools.

Category

Chemical class: First-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat respiratory tract infections caused by group A beta-hemolytic streptococci, Haemophilus influenzae, Klebsiella species, Staphylococcus aureus, and Streptococcus pneumoniae; skin and soft-tissue infections caused by S. aureus, group A beta-hemolytic and other strains of streptococci; biliary tract infections caused by Escherichia coli, Klebsiella species, Proteus mirabilis, S. aureus, and various strains of streptococci; bone and joint infections caused by S. aureus; genital infections, such as epididymitis and prostatitis, caused by E. coli, Klebsiella species, P. mirabilis, and some strains of enterococci; septicemia caused by E. coli, Klebsiella species, P. mirabilis, S. aureus, and S. pneumoniae; and endocarditis caused by group A betahemolytic streptococci and S. aureus
IV:, I.V.OR
I.M.INJECTION
Adults.For mild infections, 250 to 500 mg every 8 hr; for moderate to severe infections, 500 to 1,000 mg every 6 to 8 hr; and for severe life-threatening infections, 1,000 to 1,500 mg every 6 hr. Maximum: 6 g daily. Children: For mild to moderate infections, 25 to 50 mg/kg daily divided equally and given t.i.d. or q.i.d.; for severe infections, 100 mg/kg daily divided equally and given t.i.d. or q.i.d. To treat pneumococcal pneumonia
IV:, I.V.OR
I.M.INJECTION
Adults. 500 mg every 12 hr. To treat acute uncomplicated UTI caused by E. coli, Klebsiella species, P. mirabilis, and some strains of Enterobacter and Enterococcus
IV:, I.V.OR
I.M.INJECTION
Adults.1 g every 12 hr. To provide surgical prophylaxis
IV:, I.V.OR
I.M.INJECTION
Adults. 1 g 30 to 60 min before surgery; 0.5 to 1 g during surgery if it lasts 2 hr or longer; 0.5 to 1 g every 6 to 8 hr for 24 hr after surgery.
DOSAGE ADJUSTMENT After initial loading dose appropriate to infection’s severity, dosage interval restricted to at least 8 hr for adults with creatinine clearance of 35 to 54 ml/min/1.73 m2; dosage reduced by 50% and given every 12 hr for adults with creatinine clearance of 11 to 34 ml/min/1.73 m2; and dosage reduced by 50% and given every 18 to 24 hr for adults with creatinine clearance of 10 ml/min/1.73 m2or less. Dosage reduced to 60% and given every 12 hr for children with creatinine clearance of 40 to 70 ml/min/1.73 m2; dosage reduced to 25% and given every 12 hr for children with creatinine clearance of 20 to 40 ml/min/ 1.73 m2; and dosage reduced to 10% and given every 24 hr for children with creatinine clearance of 5 to 20 ml/min/1.73 m2.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die.

Incompatibilities

To prevent mutual inactivation, don’t mix cefazolin with aminoglycosides. Also avoid mixing cefazolin with other , including pentamidine isethionate.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Additive nephrotoxicity probenecid: Increased and prolonged blood cefazolin level

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, cefazolin sodium 185 C hepatitis, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN and serum creatinine levels, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis; injection site pain, redness, and swelling; superinfection

Cautions

Use cefazolin cautiously in patients with impaired renal function or a history of GI disease, particularly colitis. Also use cautiously in patients hypersensitive to penicillin because cross-sensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.
WARNING To prevent unintentional overdose, cefazolin for injection USP and dextrose injection USP shouldn’t be used in children who require less than the full adult dose.

Reconstitute 500-mg drug vial with 2 ml of sterile water for injection (or 1-g vial with 2.5 ml). Shake well until dissolved.

For direct I.V. injection, further dilute reconstituted solution with at least 5 ml sterile water for injection. Inject slowly over 3 to 5 minutes through tubing of a flowing compatible I.V. solution.

For intermittent I.V. infusion, reconstitute 500 to 1,000 mg in 50 to 100 ml normal saline solution, D5W, D10W, dextrose 5% in lactated Ringer’s solutoin, dextrose 5% in quarter-normal (0.2) saline solution, dextrose 5% in half-normal (0.45) saline solution, dextrose 5% in normal saline solution, lactated Ringer’s injection, 5% or 10% invert sugar in sterile water for injection, 5% sodium bicarbonate (Ancef), or Ringer’s injection.

Administer I.M injection deep into large muscle mass, such as the gluteus maximus.

Store reconstituted drug up to 24 hours at room temperature or 10 days refrigerated.

Monitor I.V. site for irritation, phlebitis, and extravasation.

Monitor BUN and serum creatinine for early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.

Be aware that an allergic reaction may occur a few days after therapy starts.

Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Watch for evidence of superinfection: cough,diarrhea,drainage,fever,malaise, pain,perineal itching,rash,redness, swelling.

Assess for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

PATIENT SAFTY

Instruct patient to complete the prescribed course of therapy.

Reassure patient that I.M. injection doesn’t typically cause pain.

Tell patient to report watery, bloody stools to prescriber immediately, even up to 2 months after drug therapy has ended.

Category

Chemical class: Cephalosporin
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat community-acquired pneumonia caused by Haemophilus influenzae (including beta-lactamase–producing strains), Haemophilus parainfluenzae (including beta-lactamase–producing strains), Streptococcus pneumoniae (penicillin-susceptible strains only), and Moraxella catarrhalis (including betalactamase–producing strains) Adults and adolescents.300 mg every 12 hr for 10 days. Maximum: 600 mg daily. To treat pharyngitis or tonsillitis caused by Streptococcus pyogenes and acute exacerbations of chronic bronchitis caused by H. influenzae (including beta-lactamase–producing strains), H. parainfluenzae (including betalactamase–producing strains), S. pneucefdinir 186 moniae (penicillin-susceptible strains only), and M. catarrhalis (including beta-lactamase–producing strains) Adults and adolescents.300 mg every 12 hr for 5 to 10 days or 600 mg every 24 hr for 10 days. Maximum: 600 mg daily. ORAL SUSPENSION Children ages 6 months to 12 years. 7 mg/ kg every 12 hr for 5 to 10 days or 14 mg/kg every 24 hr for 10 days (for pharyngitis or tonsillitis). To treat acute maxillary sinusitis caused by H. influenzae (including betalactamase–producing strains), S. pneumoniae (penicillin-susceptible strains only), and M. catarrhalis (including beta-lactamase–producing strains) Adults and adolescents. 300 mg every 12 hr or 600 mg every 24 hr for 10 days. Maximum: 600 mg daily. ORAL SUSPENSION Children ages 6 months to 12 years. 7 mg/ kg every 12 hr or 14 mg/kg every 24 hr for 10 days. To treat uncomplicated skin and softtissue infections caused by Staphylococcus aureus (including betalactamase–producing strains) and Streptococcus pyogenes Adults and adolescents.300 mg every 12 hr for 10 days. Maximum: 600 mg daily. ORAL SUSPENSION Children ages 6 months to 12 years. 7 mg/ kg every 12 hr for 10 days. To treat acute bacterial otitis media caused by H. influenzae (including beta-lactamase–producing strains), S. pneumoniae (penicillin-susceptible strains only), and M. catarrhalis (including beta-lactamase–producing strains) ORAL SUSPENSION Children ages 6 months to 12 years. 7 mg/ kg every 12 hr for 5 to 10 days or 14 mg/kg every 24 hr for 10 days.
DOSAGE ADJUSTMENT For adults with creatinine clearance less than 30 ml/min/1.73 m2, expect to reduce cefdinir dosage to 300 mg daily; for children with creatinine clearance less than 30 ml/min/1.73 m2, dosage is 7 mg/kg (up to 300 mg) daily. For patients undergoing intermittent hemodialysis, dosage is 300 mg or 7 mg/kg every other day, beginning at the end of each hemodialysis session, as prescribed.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die. Because cefdinir is not degraded by some bacterial beta-lactamase enzymes, it’s effective against many organisms that are resistant to both penicillins and some cephalosporins.

Contraindications

Hypersensitivity to cefdinir, other cephalosporins, or their components

Interactions

antacids that contain aluminum or magnesium: Decreased cefdinir absorption if given within 2 hours of antacid iron salts: Reduced cefdinir absorption if given within 2 hours of iron probenecid: Increased blood level and prolonged half-life of cefdinir

Side Efect

CNS: Asthenia, dizziness, drowsiness, headache, insomnia, somnolence
EENT: Dry mouth, pharyngitis, rhinitis
GI: Abdominal pain, anorexia, constipation, diarrhea, flatulence, indigestion, nausea, pseudomembranous colitis, stool discoloration, vomiting GU:Leukorrhea,vaginal candidiasis,vaginitis
HEME: Leukopenia
SKIN: Pruritus, rash
Other: Anaphylaxis, serum sicknesslike reaction

Cautions

To reconstitute cefdinir powder for oral suspension, tap bottle to loosen powder, and then dilute with water to 125 mg/ 5 ml. Shake well before each use. Discard any unused portion after 10 days. Keep suspension bottle tightly closed, and store it at room temperature.

Give antacids that contain aluminum or magnesium and iron salts at least 2 hours before or after cefdinir because they may cefdinir 187 C interfere with cefdinir absorption.

Monitor patient allergic to penicillin for evidence of hypersensitivity reaction, from a mild rash to fatal anaphylaxis, because cross-sensitivity can occur.

Monitor patient with a chronic GI condition, such as colitis, for signs and symptoms of a drug-related exacerbation.

Because all cephalosporins have the potential to cause bleeding, monitor elderly patients and patients with a preexisting coagulopathy, including vitamin K deficiency, for elevated PT or APTT.

Monitor patient closely for diarrhea, which may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold cefdinir and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Assess for other evidence of superinfection, including perineal itching; loose, foul-smelling stools; and vaginal drainage.

PATIENT SAFTY

Advise patient taking cefdinir oral suspension to shake bottle well before use and to use a liquid-measuring device to ensure accurate dose.

Inform patient that tablet coating may cause stools to become a reddish color.

Instruct patient to complete entire course of therapy, even if he feels better.

Advise patient to take iron salts and aluminumor magnesium-containing antacids at least 2 hours before or after taking cefdinir.

Inform patient with history of colitis that cefdinir may worsen it; urge him to notify prescriber promptly if symptoms develop.

Inform patient with diabetes mellitus that oral suspension contains 2.86 g of sucrose per teaspoon; advise him to monitor his blood glucose levels as appropriate.

Teach patient to recognize and report evidence of superinfection, such as perineal itching; loose, foul-smelling stools; and vaginal drainage.

Inform patient that yogurt and buttermilk can help prevent superinfection and may decrease diarrhea.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and can be serious, requiring prompt treatment.

Category

Chemical class: Cephalosporin
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat mild to moderate acute bacterial exacerbation of chronic bronchitis or community-acquired pneumonia caused by Haemophilus influenzae (including beta-lactamase–producing strains), Haemophilus parainfluenzae (including beta-lactamase–producing strains), Streptococcus pneumoniae (penicillinsusceptible strains), or Moraxella catarrhalis (including betalactamase–producing strains) Adults and children age 12 and over. 400 mg b.i.d. for 10 days or for 14 days for community-acquired pneumonia. To treat mild to moderate pharyngitis and tonsillitis caused by Streptococcus pyogenes Adults and children age 12 and over. 200 mg b.i.d. for 10 days. To treat mild to moderate uncomplicated skin and soft-tissue infections caused by Staphylococcus aureus (including beta-lactamase–producing strains) or S. pyogenes Adults and children age 12 and over. 200 mg b.i.d. for 10 days.
DOSAGE ADJUSTMENT Inmoderate renal impairment (creatinine clearance 30 to 49 ml/min/1.73 m2), maximum dosage reduced to 200 mg b.i.d. In severe renal impairment (creatinine clearance less than 30 ml/min/1.73 m2), maximum dosage reduced to 200 mg daily.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidocefditoren pivoxil 188 glycan makes the cell membrane rigid and protective. Without it, bacterial cells rupture and die. This

Mechanism of Action

is most effective against bacteria that divide rapidly, including many gram-positive and gram-negative bacteria. Cefditoren isn't inactivated by beta lactamase produced by some bacteria.

Contraindications

Carnitine deficiency or inborn metabolic disorder that causes it; hypersensitivity to cephalosporins or their components

Interactions

aluminumand magnesium-containing antacids, H2-receptor antagonists: Reduced cefditoren absorption probenecid: Increased and prolonged blood cefditoren level food: Increased cefditoren absorption

Side Efect

CNS: Headache, hyperactivity, hypertonia, seizures
GI: Abdominal pain, diarrhea, dyspepsia, hepatic dysfunction, nausea, pseudomembranous colitis, vomiting
GU: Acute renal failure, renal dysfunction, toxic nephropathy
HEME: Aplastic anemia, hemolytic anemia, hemorrhage, thrombocytopenia
MS: Arthralgia
RESP: Pneumonia
SKIN: Erythema multiforme, StevensJohnson syndrome, toxic epidermal necrolysis
Other: Allergic reaction, anaphylaxis, carnitine deficiency, drug fever, serum sicknesslike reaction, superinfection

Cautions

WARNING Before starting cefditoren therapy, determine if patient is hypersensitive to milk protein because cefditoren contains sodium caseinate, a milk protein. Drug should not be given to patient with this hypersensitivity. Also determine if patient has had a hypersensitivity reaction to cefditoren or other cephalosporins (because drug is contraindicated in these patients) or to penicillin (because crosssensitivity has occurred in about 10% of such patients).

Cefditoren shouldn’t be used for prolonged treatment because of the risk of carnitine deficiency.

If possible, obtain culture and sensitivity test results before giving cefditoren.

Assess patient for evidence of Clostridium difficile infection and pseudomembranous colitis, such as profuse, watery diarrhea. For mild cases, expect to discontinue cefditoren. For moderate to severe cases, expect to also give fluids and electrolytes, protein supplementation, and an antibacterial drug effective against C. difficile.

If an allergic reaction occurs, expect to discontinue drug, as prescribed. For serious acute hypersensitivity reactions, expect to also give epinephrine, oxygen, and I.V. fluids, antihistamines, corticosteroids, and vasopressors, as prescribed.

Monitor BUN and serum creatinine levels to detect early signs of renal dysfunction. Also monitor fluid intake and output.

Watch for a decreased PT, as ordered, in at-risk patients, such as those with renal or hepatic impairment, those with a poor nutritional state, and those receiving anticoagulant or prolonged antibiotic therapy. Notify prescriber if a decrease occurs, and give vitamin K as ordered.

PATIENT SAFTY

Urge patient to complete prescribed course of therapy.

Instruct patient to take cefditoren with meals to enhance drug absorption.

Advise patient not to take cefditoren with aluminumor magnesium-containing antacids or other used to reduce stomach acids because these may interfere with cefditoren absorption.

Explain that yogurt and buttermilk help maintain normal intestinal flora and can decrease diarrhea during therapy.

Instruct patient to immediately report severe diarrhea to prescriber.

Category

Chemical class: Fourth-generation cephalocefepime hydrochloride 189 C sporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat mild to moderate UTI caused by Escherichia coli, Klebsiella pneumoniae, or Proteus mirabilis
IV:,
I.M.INJECTION(ONLY FOR UTI CAUSED BY E.COLI) Adults and children age 12 and over.500 to 1,000 mg every 12 hr for 7 to 10 days. To treat severe UTI caused by E. coli or K. pneumoniae, moderate to severe skin and soft-tissue infections caused by Staphylococcus aureus or Streptococcus pyogenes
IV: Adults and children age 12 and over.2 g every 12 hr for 10 days. To treat moderate to severe pneumonia caused by Enterobacter species, K. pneumoniae, Pseudomonas aeruginosa, or Streptococcus pneumoniae
IV: Adults and children age 12 and over.1 to 2 g every 12 hr for 10 days. To treat febrile neutropenia
IV: Adults and children age 12 and over. 2 g every 8 hr for 7 days or until neutropenia resolves. To treat complicated intra-abdominal infections (together with metronidazole) caused by alpha-hemolytic streptococci, Bacteroides fragilis, E. coli, Enterobacter species, K. pneumoniae, or P. aeruginosa
IV: Adults and children age 12 and over.2 g every 12 hr for 7 to 10 days.
DOSAGE ADJUSTMENT Dosing interval increased from 12 to 24 hr and from 8 to 12 hr if creatinine clearance is 30 to 60 ml/ min/1.73 m2. Interval increased from 8 or 12 hr to 24 hr and dose decreased from 2 g every 12 hr to 1 g every 24 hr (all other doses unchanged) if creatinine clearance is 11 to 29 ml/min/1.73 m2. Dosage decreased from 500 mg every 12 hr to 250 mg every 24 hr, from 1,000 mg every 12 hr to 250 mg every 24 hr, from 2,000 mg every 12 hr to 500 mg every 24 hr, and from 2 g every 8 hr to 1 g every 24 hr if creatinine clearance is less than 11 ml/min/1.73 m2.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die.

Incompatibilities

Don’t add cefepime to solutions that contain ampicillin in a concentration of more than 40 mg/ml. Don’t add drug to solutions that contain aminophylline, gentamycin, metronidazole, netilmicin sulfate, tobramycin, or vancomycin.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of renal failure in renal disease

Side Efect

CNS: Chills, coma, confusion, fever, hallucinations, headache, myoclonus, seizures, stupor
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis; injection site pain, redness, and swelling; superinfection

Cautions

Use cefepime cautiously in patients with impaired renal function or a history of GI disease, particularly colitis. Also use cautiously in patients hypersensitive to penicillin because cross-sensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug. cefepime hydrochloride 190

For I.V. infusion, reconstitute using manufacturer’s guidelines. Give over 30 minutes.

For I.M. injection, reconstitute 500-mg vial of drug with 1.3 ml of diluent, such as sterile water for injection (or 1-g vial with 2.4 ml of diluent). See drug guidelines for complete list of appropriate diluents.

Be aware that an allergic reaction may occur a few days after therapy starts.

Monitor BUN and serum creatinine levels for early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity. Be aware that unadjusted dosages of cefepime in renally impaired patients may cause myoclonus and seizures.

Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Assess for signs of superinfection, such as perineal itching, fever, malaise, redness, pain, swelling, drainage, rash, diarrhea, and cough or sputum changes.

Assess for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

Monitor patient for evidence of encepalopathy, such as changes in level of consciousness, myoclonus, and seizures. Patient will need immediate treatment, and the cefepime dosage will need to be adjusted or the drug discontinued.

PATIENT SAFTY

Tell patient to immediately report severe diarrhea to prescriber.

Instruct patient and caregiver to immediately seek emergency care for any change in mental status, such as coma, hallucinations, decreased responsiveness, abnormal movements, or seizures. Cefepime should be stopped until patient is evaluated.

Category

Chemical class: Third-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat uncomplicated UTI caused by Escherichia coli and Proteus mirabilis; otitis media caused by Haemophilus influenzae, Moraxella catarrhalis, or Streptococcus pyogenes; pharyngitis and tonsillitis caused by S. pyogenes; acute bronchitis and acute exacerbations of chronic bronchitis caused by H. influenzae and Streptococcus pneumoniae ORAL SUSPENSION Children.8 mg/kg daily or 4 mg/kg every 12 hr. Adults and children over 50 kg (110 lb) or age 12. 400 mg daily or 200 mg every 12 hr. To treat uncomplicated gonorrhea caused by Neisseria gonorrhoeae Adults and children over 50 kg or age 12. 400 mg daily.
DOSAGE ADJUSTMENT Dosage reduced to 75% for patients who have creatinine clearance of 21 to 60 ml/min/1.73 m2or receive hemodialysis. Dosage reduced to 50% for patients who have creatinine clearance of 20 ml/min/1.73 m2or less.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity carbamazepine: Increased blood carbamazepine level

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatitis, hepatomegaly, jaundice, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis cefixime 191 C
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, angioedema, facial edema, superinfection

Cautions

Use cefixime cautiously in patients with impaired renal function or a history of GI disease, especially colitis. Also use cautiously in patients hypersensitive to penicillin because cross-sensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

Tablets shouldn’t be substituted for oral suspension to treat otitis media because cefixime suspension produces a higher peak blood level than do tablets when administered at the same dose.

Monitor BUN and serum creatinine for early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.

Be aware that an allergic reaction may occur a few days after therapy starts.

Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Assess for signs of superinfection, such as perineal itching, fever, malaise, redness, pain, swelling, drainage, rash, diarrhea, and cough or sputum changes.

Assess for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

PATIENT SAFTY

Instruct patient to complete the prescribed course of therapy.

Advise patient to shake oral suspension well before pouring dose and to use a calibrated device to obtain an accurate dose.

Instruct patient to store oral suspension at room temperature and to discard unused portion after 14 days.

Tell patient to immediately report severe diarrhea to prescriber.

Inform patient that yogurt and buttermilk can help maintain intestinal flora and decrease diarrhea.

Teach patient to recognize and report signs of superinfection, such as furry tongue, perineal itching, and loose, foulsmelling stools.

Category

Chemical class: Second-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat UTI caused by Escherichia coli; lower respiratory tract infections, such as bronchitis and pneumonia, caused by E. coli, Haemophilus influenzae, Staphylococcus aureus, and Streptococcus pneumoniae; skin and soft-tissue infections caused by Bacteroides fragilis, Bacteroides melaninogenicus, E. coli, Klebsiella oxytoca, Klebsiella pneumoniae, Morganella morganii, Proteus mirabilis, Proteus vulgaris, S. aureus, Staphylococcus epidermidis, Streptococcus agalactiae, and Streptococcus pyogenes; intra-abdominal infections caused by B. fragilis, Clostridium perfringens, E. coli, K. oxytoca, and K. pneumoniae
IV:
Adults.2 g every 6 to 12 hr for 5 to 14 days.
DOSAGE ADJUSTMENT Dosage reduced to 1 to 2 g every 12 hr if creatinine clearance is 50 to 90 ml/min/1.73 m2; 1 to 2 g every 16 hr if creatinine clearance is 30 to 49 ml/ min/1.73 m2; 1 to 2 g every 24 hr if creatinine clearance is 10 to 29 ml/min/1.73 m2; and 1 to 2 g every 48 hr if creatinine clearance is less than 10 ml/min/1.73 m2. To provide surgical prophylaxis for vaginal hysterectomy
IV:
Adults. 2 g as a single dose 30 to 90 min before surgery or 1 g 30 to 90 min before surgery and repeated 8 and 16 hr later. To provide surgical prophylaxis for abdominal hysterectomy and for highrisk cholecystectomy
IV: cefmetazole sodium 192
Adults. 1 g 30 to 90 min before surgery and repeated 8 and 16 hr later. To provide surgical prophylaxis for cesarean section
IV:
Adults. 2 g as a single dose after cord is clamped or 1 g after cord is clamped and then repeated 8 and 16 hr later. To provide surgical prophylaxis for colorectal surgery
IV:
Adults. 2 g as a single dose 30 to 90 min before surgery or 2 g 30 to 90 min before surgery and repeated 8 and 16 hr later.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity anticoagulants: Possibly increased anticoagulant effect probenecid: Increased and prolonged blood cefmetazole level
alcohol use: Possibly disulfiram-like reaction

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis; injection site pain, redness, and swelling; superinfection

Cautions

Use cefmetazole cautiously in patients hypersensitive to penicillin; cross-sensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

Reconstitute drug with sterile or bacteriostatic water for injection or sodium chloride for injection.

Dilute primary solution as needed to 1 to 20 mg/ml in D5W, normal saline solution, lactated Ringer’s solution, or 1% lidocaine solution without epinephrine.

Store reconstituted solution for up to 24 hours at room temperature or 7 days refrigerated.

Monitor BUN and serum creatinine levels and fluid intake and output to detect early signs of nephrotoxicity.

Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Assess for signs of superinfection, such as perineal itching, fever, malaise, redness, rash, diarrhea, and cough or sputum changes.

Assess for pharyngitis, bleeding, and arthralgia, which may indicate blood dyscrasia. Monitor PT and bleeding time, as ordered.

PATIENT SAFTY

Advise patient to immediately report severe diarrhea to prescriber.

Instruct patient to avoid alcohol during therapy and for at least 3 days after last dose.

Category

Chemical class: Second-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat lower respiratory tract infections caused by Escherichia coli, Haemophilus influenzae, Klebsiella cefonicid sodium 193 C pneumoniae, and Streptococcus pneumoniae; UTI caused by E. coli, K. pneumoniae, Morganella morganii, Proteus mirabilis, Proteus vulgaris, and Providencia rettgeri; skin and soft-tissue infections caused by Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus agalactiae, and Streptococcus pyogenes; septicemia caused by E. coli and S. pneumoniae; and bone and joint infections caused by S. aureus
IV:, I.V.OR
I.M.INJECTION
Adults. For mild to moderate infections, 1 g every 24 hr. For severe or life-threatening infections, 2 g every 24 hr. To treat uncomplicated UTI
IV:, I.V.OR
I.M.INJECTION
Adults.500 mg every 24 hr.
DOSAGE ADJUSTMENT Initial dose reduced to 75 mg/kg I.V. or I.M. in patients with impaired renal function. Then reduced to 10 to 25 mg/kg every 24 hr if creatinine clearance is 60 to 79 ml/min/1.73 m2; 8 to 20 mg/kg every 24 hr if creatinine clearance is 40 to 59 ml/min/1.73 m2; 4 to 15 mg/kg every 24 hr if creatinine clearance is 20 to 39 ml/min/1.73 m2; 4 to 15 mg/kg every 48 hr if creatinine clearance is 10 to 19 ml/ min/1.73 m2; 4 to 15 mg/kg every 3 to 5 days if creatinine clearance is 5 to 9 ml/ min/1.73 m2; and 3 to 4 mg/kg every 3 to 5 days if creatinine clearance is less than 5 ml/min/1.73 m2. To provide surgical prophylaxis
IV:, I.V.OR
I.M.INJECTION
Adults. 1 g 60 min before surgery. Dose repeated once daily, if needed, for 2 days after prosthetic arthroplasty or open-heart surgery.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die.

Incompatibilities

To prevent mutual inactivation, don’t mix cefonicid with aminoglycosides.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis; injection site pain, redness, and swelling; superinfection

Cautions

Use cefonicid cautiously in patients with impaired renal function. Also use cautiously in patients hypersensitive to penicillin because cross-sensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

Reconstitute each 500-mg vial of drug with 2 ml sterile water for injection (or each 1-g vial with 2.5 ml).

For I.V. infusion, dilute further in 50 to 100 ml compatible solution, such as D5W, D10W, dextrose 5% in quarter-normal (0.2) saline solution, dextrose 5% in halfnormal (0.45) saline solution, or dextrose 5% in normal saline solution.

Give I.V. injection slowly over 3 to 5 minutes through tubing of a flowing compatible I.V. solution.

For I.M. dose larger than 1 g, divide dose in half and give into large muscle mass, such as the gluteus maximus, at two different sites.

Reconstituted solution may be stored 24 hours at room temperature, 72 hours refrigerated.

Monitor patient’s BUN and serum creatinine levels to detect early signs of nephrocefonicid sodium 194 toxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.

Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Watch for evidence of superinfection, such as perineal itching, fever, malaise, redness, pain, swelling, drainage, rash, diarrhea, and cough or sputum changes.

Assess patient for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

PATIENT SAFTY

Warn patient that I.M. injection may be painful.

Tell patient to immediately report severe diarrhea to prescriber.

Category

Chemical class: Third-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat respiratory tract infections caused by Enterobacter species, Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, and other streptococci (excluding enterococci); UTI caused by E. coli and P. aeruginosa; uncomplicated gonorrhea caused by Neisseria gonorrhoeae; gynecologic infections caused by anaerobic gram-positive cocci, Bacteroides species, Clostridium species, E. coli, Staphylococcus epidermidis, and Streptococcus agalactiae; bacterial septicemia caused by E. coli, Klebsiella species, S. aureus, Serratia marcescens, and streptococci; skin and soft-tissue infections caused by P. aeruginosa, S. aureus, and S. pyogenes; and intraabdominal infections caused by anaerobic gram-negative bacilli, E. coli, and P. aeruginosa
IV:,
I.M.INJECTION
Adults.1 to 2 g every 12 hr. For severe infections or those caused by less sensitive organisms, 6 to 12 g daily divided into equal doses and given b.i.d., t.i.d., or q.i.d. Maximum: 12 g daily.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die.

Incompatibilities

To prevent mutual inactivation, don’t mix cefoperazone with aminoglycosides. Also avoid mixing cefoperazone with other , including pentamidine isethionate.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity oral anticoagulants, other that affect blood clotting: Increased anticoagulant effect
alcohol use: Disulfiram-like reaction

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis; injection site pain, redness, and swelling; superinfection cefoperazone sodium 195 C

Cautions

Use cefoperazone cautiously in patients with a history of bleeding problems, GI disease (especially colitis), or severely impaired hepatic or renal function. Also use cautiously in patients hypersensitive to penicillin because cross-sensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

For I.V. use, reconstitute with required amount of diluent. Then further dilute in compatible solution, such as D5W, D10W, dextrose 5% in lactated Ringer’s solution, dextrose 5% in quarter-normal (0.2) saline solution, dextrose 5% in normal saline solution, lactated Ringer’s injection, normal saline solution, Normosol M and D5W, or Normosol R. (See manufacturer’s guidelines for details.)

Give I.V. drug as intermittent infusion over 15 to 30 minutes or as continuous infusion. Direct bolus injection isn’t recommended.

For I.M. injection, reconstitute drug with bacteriostatic water for injection (that contains benzyl alcohol or parabens) or sterile water for injection.

After reconstitution, let foam dissipate, and inspect the solution to ensure complete dissolution.

Store reconstituted solution at room temperature for 24 hours.

Monitor BUN and serum creatinine levels to detect early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.

Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Assess for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

Assess for evidence of superinfection, such as perineal itching, fever, malaise, redness, pain, swelling, drainage, rash, diarrhea, and cough or sputum changes.

PATIENT SAFTY

Advise patient to avoid alcohol during therapy and for at least 3 days after last dose.

Explain that I.M. injection may hurt.

Tell patient to immediately report severe diarrhea to prescriber.

Category

Chemical class: Third-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To provide perioperative prophylaxis
IV:, I.V.OR
I.M.INJECTION Adults and children weighing more than 50 kg (110 lb). 1 g 30 to 90 min before surgery. To provide perioperative prophylaxis related to cesarean section
IV:, I.V.OR
I.M.INJECTION
Adults. 1 g as soon as cord is clamped, then 1 g every 6 hr for up to two doses. To treat gonococcal urethritis and cervicitis in men and women
I.M.INJECTION Adults weighing more than 50 kg. 500 mg as a single dose. To treat rectal gonorrhea in women
I.M.INJECTION Adults weighing more than 50 kg. 500 mg as a single dose. To treat rectal gonorrhea in men
I.M.INJECTION Adults weighing more than 50 kg. 1 g as a single dose. To treat disseminated gonorrhea
IV: OR INJECTION Adults and children weighing more than 50 kg. 1 g every 8 hr. To treat uncomplicated infections caused by susceptible organisms
IV:, I.V.OR
I.M.INJECTION Adults and children weighing more than 50 kg. 1 g every 12 hr. Children ages 1 month to 12 years weighing less than 50 kg. 50 to 180 mg/kg daily in four to six divided doses. Children ages 1 to 4 weeks.50 mg/kg I.V. every 8 hr. Children age 1 week and under. 50 mg/kg I.V. every 12 hr. To treat moderate to severe infections caused by susceptible organisms
IV:, I.V.OR
I.M.INJECTION Adults and children weighing more than cefotaxime sodium 196 50 kg. 1 to 2 g every 8 hr. Children ages 1 month to 12 years weighing less than 50 kg. 50 to 180 mg/kg daily in four to six divided doses. For more serious infections, including meningitis, higher dosages are used. Children ages 1 to 4 weeks.50 mg/kg I.V. every 8 hr. Children age 1 week and younger.50 mg/ kg I.V. every 12 hr. To treat septicemia and other infections that commonly require antibiotics in higher doses than those used to treat moderate to severe infections
IV: OR INJECTION Adults and children weighing more than 50 kg. 2 g every 6 to 8 hr. To treat life-threatening infections caused by susceptible organisms
IV: OR INJECTION Adults and children weighing more than 50 kg. 2 g every 4 hr. Maximum: 12 g daily. Children ages 1 month to 12 years weighing less than 50 kg. 50 to 180 mg/kg daily in four to six divided doses. Children ages 1 to 4 weeks.50 mg/kg every 8 hr. Children age 1 week and younger.50 mg/ kg every 12 hr.
DOSAGE ADJUSTMENT Dosage reduced by 50% for patients with estimated creatinine clearance below 20 ml/min/1.73 m2.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting cross-linking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die.

Incompatibilities

To prevent mutual inactivation, don’t mix cefotaxime with aminoglycosides. Also avoid mixing cefotaxime with other , including pentamidine isethionate.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity probenecid: Increased and prolonged blood cefotaxime level

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, cholestasis, diarrhea, elevated liver function test results, hepatic failure, hepatitis, hepatomegaly, jaundice, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis; injection site pain, redness, and swelling; superinfection

Cautions

Use cefotaxime cautiously in patients with impaired renal function, a history of GI disease (especially colitis), or hypersensitivity to penicillin because cross-sensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

For I.V. use, reconstitute each 0.5-, 1-, or 2-g vial with 10 ml of sterile water for injection. Shake to dissolve.

For intermittent I.V. infusion, further dilute in 50 to 100 ml of D5W or normal saline solution.

For I.M. use, reconstitute each 500-mg vial with 2 ml sterile water for injection or bacteriostatic water for injection; each 1-g vial with 3 ml diluent; and each 2-g vial with 5 ml diluent. Shake to dissolve.
WARNING When preparing drug for a neonate, don’t use diluent that contains benzyl alcohol; it could cause a fatal toxic syndrome.

Give cefotaxime by I.V. injection over 3 to 5 minutes through tubing of a free-flowing compatible I.V. solution. Temporarily stop other solutions being given through same I.V. site.

Discard unused drug after 24 hours if stored at room temperature, 5 days if refrigerated. cefotaxime sodium 197 C

Protect cefotaxime powder and solution from light and heat.

Monitor I.V. sites for signs of phlebitis or extravasation. Rotate I.V. sites every 72 hours.

Monitor BUN and serum creatinine levels and fluid intake and output for signs of nephrotoxicity.

Be aware that allergic reaction may occur a few days after cefotaxime therapy starts.

Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold cefotaxime and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Assess patient for pharyngitis, ecchymosis, bleeding, and arthralgia, which may indicate a blood dyscrasia. Monitor CBC, PT, and bleeding time, as ordered.

Monitor patient closely for superinfection. If evidence appears, notify prescriber and expect to stop drug and provide care.

PATIENT SAFTY

Explain that I.M. injection may be painful.

Instruct patient to report watery, bloody stools to prescriber immediately, even up to 2 months after drug therapy has ended.

Category

Chemical class: Second-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To provide surgical prophylaxis I.V. INJECTION
Adults. 1 to 2 g 30 to 60 min before surgery or, in cesarean section, as soon as cord is clamped. To treat lower respiratory tract infections caused by Escherichia coli, Haemophilus influenzae, Klebsiella species, Proteus mirabilis, Serratia marcescens, Staphylococcus aureus, and Streptococcus pneumoniae; gynecologic infections caused by Bacteroides species (excluding B. distasonis, B. ovatus, and B. thetaiotaomicron), E. coli, Fusobacterium species, gram-positive anaerobic cocci, Neisseria gonorrhoeae, P. mirabilis, S. aureus, Staphylococcus epidermidis, and Streptococcus species (excluding enterococci); intra-abdominal infections caused by Bacteroides species (excluding B. distasonis, B. ovatus, and B. thetaiotaomicron), Clostridium species, E. coli, Klebsiella species, and Streptococcus species (excluding enterococci); and bone and joint infections caused by S. aureus

IV

, I.V. OR

IM

Adults.For mild to moderate infections, 1 to 2 g every 12 hr.

IV

OR INJECTION
Adults.For severe infections, 2 g every 12 hr; for life-threatening infections, 3 g every 12 hr. To treat UTI caused by E. coli, Klebsiella species, or Proteus species

IV

, I.V. OR

IM

Adults. 0.5 to 2 g every 12 hr or 1 to 2 g every 24 hr. To treat skin and soft-tissue infections caused by E. coli, Klebsiella pneumoniae, Peptostreptococcus species, S. aureus, S. epidermidis, Streptococcus pyogenes, and Streptococcus species (excluding enterococci)

IV

, I.V. OR

IM

Adults. For mild to moderate infections due to K. pneumoniae, 1 or 2 g every 12 hr. For mild to moderate infections caused by other organisms, 1 g I.M. or I.V. every 12 hr or 2 g I.V. every 24 hr; for severe infections, 2 g I.V. every 12 hr.
DOSAGE ADJUSTMENT Dosing interval reduced to 24 hr if creatinine clearance is 10 to 30 ml/min/1.73 m2and to 48 hr if creatinine clearance is less than 10 ml/min/ 1.73 m2.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die.

Incompatibilities

To prevent mutual inactivation, don’t mix cefotetan with aminoglycosides. cefotetan disodium 198

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity oral anticoagulants, other that affect blood clotting: Enhanced anticoagulant effect probenecid: Increased and prolonged blood cefotetan level
alcohol use: Disulfiram-like reaction

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis; injection site pain, redness, and swelling; superinfection

Cautions

Use cefotetan cautiously in patients with impaired renal function or a history of GI disease, especially colitis. Also use cautiously in patients hypersensitive to penicillin because cross-sensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

For I.V. use, reconstitute each 1-g vial of drug with 10 ml sterile water for injection. For each 2-g vial, use 10 to 20 ml diluent. For I.V. infusion, further dilute solution in 50 to 100 ml D5W or normal saline solution.

For direct I.V. injection, give drug slowly over 3 to 5 minutes through tubing of a flowing compatible I.V. solution.

For I.M. use, reconstitute each 1-g vial of drug with 2 ml of sterile or bacteriostatic water for injection, or sodium chloride for injection. For a 2-g vial, use 3 ml diluent.

Monitor I.V. site for signs and symptoms of phlebitis and extravasation; rotate sites every 72 hours.

Protect reconstituted solution from light, and store for up to 24 hours at room temperature or 96 hours under refrigeration.

Be aware than an allergic reaction may occur a few days after therapy starts.

Monitor BUN and serum creatinine levels and fluid intake and output for signs of nephrotoxicity.

Monitor patient receiving even short-term cefotetan therapy for signs and symptoms of hemolytic anemia, such as marked pallor and fatigue.

If patient receives long-term therapy, monitor CBC and serum AST, ALT, bilirubin, LD, and alkaline phosphatase levels.

Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Watch for pharyngitis, ecchymosis, bleeding, and arthralgia, which may indicate a blood dyscrasia. Monitor PT and bleeding time, as ordered. Be prepared to give vitamin K, if ordered, to treat hypoprothrombinemia.

PATIENT SAFTY

Explain that I.M. injection may be painful.

Tell patient to immediately report severe diarrhea to prescriber.

Urge patient to avoid alcohol during and for at least 3 days after cefotetan therapy.

Category

Chemical class: Second-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To provide surgical prophylaxis

IV

OR INJECTION
Adults.2 g 30 to 60 min before surgery and then 2 g every 6 hr after first dose for up to 24 hr. cefoxitin sodium 199 C Children age 3 months or over. 30 to 40 mg/kg 30 to 60 min before surgery and every 6 hr after first dose for up to 24 hr. To provide surgical prophylaxis for cesarean section

IV

OR INJECTION
Adults. 2 g as a single dose as soon as cord is clamped or 2 g as soon as cord is clamped followed by 2 g 4 and 8 hr after initial dose. To provide surgical prophylaxis for transurethral prostatectomy

IV

OR INJECTION
Adults.1 g 30 to 60 min before surgery and then 1 g every 8 hr for up to 5 days. To treat infections, including septicemia, gynecologic infections, intra-abdominal infections, UTI, and infections of the lower respiratory tract, skin, soft tissue, bones, and joints caused by anaerobes (including Bacteroides species, Clostridium species, Fusobacterium species, Peptococcus niger, and Peptostreptococcus species), gramnegative organisms (including Escherichia coli, Haemophilus influenzae [also ampicillin-resistant strains], Klebsiella, and Proteus species), and gram-positive organisms (including Staphylococcus aureus [penicillinaseand non–penicillinase-producing strains], Staphylococcus epidermidis, Streptococcus agalactiae, Streptococcus pneumoniae, and Streptococcus pyogenes)
IV: OR INJECTION
Adults. For uncomplicated infections, 1 g every 6 to 8 hr; for moderate to severe infections, 1 g every 4 hr or 2 g every 6 to 8 hr. For infections that commonly require high-dose antibiotics (such as gas gangrene), 2 g every 4 hr or 3 g every 6 hr. Children age 3 months or over. 80 to 160 mg/kg daily in equal doses given every 4 to 6 hr (higher dosages used for more severe infections). Maximum: 12 g daily. To treat uncomplicated gonorrhea
I.M.INJECTION
Adults. 2 g as a single dose along with 1 g oral probenecid concurrently or within 30 min of cefoxitin.
DOSAGE ADJUSTMENT Dosage reduced to 1 to 2 g every 8 to 12 hr if creatinine clearance is 30 to 50 ml/min/1.73 m2; 1 to 2 g every 12 to 24 hr if clearance is 10 to 29 ml/ min/1.73 m2; 0.5 to 1 g every 12 to 24 hr if clearance is 5 to 9 ml/min/1.73 m2; and 0.5 to 1 g every 24 to 48 hr if clearance is less than 5 ml/min/1.73 m2.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die.

Incompatibilities

To prevent mutual inactivation, don’t mix cefoxitin with aminoglycosides. Also avoid mixing cefoxitin with other , including pentamidine isethionate.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, flushing, pruritus, rash, Stevens-Johnson syndrome, urticaria
Other: Anaphylaxis; injection site pain, redness, and swelling; superinfection

Cautions

Use cefoxitin cautiously in patients hypersensitive to penicillin; cross-sensitivity has occurred in about 10% of such patients.

Also use cautiously in patients with a history of GI disease, particularly colitis, because of an increased risk of cefoxitin sodium 200 pseudomembranous colitis.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

For I.V. use, reconstitute 1 g with 10 ml sterile water for injection or 2 g with 10 to 20 ml diluent.

For I.V. injection, give slowly over 3 to 5 minutes through tubing of a flowing compatible I.V. solution.

For intermittent infusion, further dilute with 50 to 100 ml D5W or normal saline solution.

For continuous high-dose infusion, add cefoxitin to I.V. solutions of D5W, normal saline solution, or dextrose 5% in normal saline solution.

For I.M. use, reconstitute each 1 g with 2 ml sterile water for injection.

Discard unused drug after 24 hours if stored at room temperature or after 1 week if refrigerated.

Be aware that powder or solution may darken during storage, which doesn’t reflect altered potency.

Be aware that an allergic reaction may occur a few days after therapy starts.

Monitor BUN and serum creatinine for early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.

Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Assess for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

PATIENT SAFTY

Tell patient to immediately report severe diarrhea to prescriber.

Instruct patient to complete the course of therapy as prescribed.

Category

Chemical class: Third-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat acute community-acquired pneumonia caused by Haemophilus influenzae or Streptococcus pneumoniae ORAL SUSPENSION, Adults and adolescents over age 13. 200 mg every 12 hr for 14 days. To treat acute bacterial exacerbation of chronic bronchitis caused by H. influenzae, Moraxella catarrhalis, or S. pneumoniae Adults and adolescents over age 13. 200 mg every 12 hr for 10 days. To treat uncomplicated gonorrhea in men and women and rectal gonococcal infections in women caused by Neisseria gonorrhoeae ORAL SUSPENSION,
Adults. 200 mg as a single dose. To treat uncomplicated UTI caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, or Staphylococcus saprophyticus ORAL SUSPENSION,
Adults.100 mg every 12 hr for 7 days. To treat skin and soft-tissue infections caused by Staphylococcus aureus or Staphylococcus pyogenes ORAL SUSPENSION, Adults and adolescents over age 13. 400 mg every 12 hr for 7 to 14 days. To treat acute otitis media caused by H. influenzae, M. catarrhalis, or S. pneumoniae ORAL SUSPENSION, Children ages 5 months through 12 years. 5 mg/kg every 12 hr (maximum: 200 mg/ dose) or 10 mg/kg every 24 hr (maximum: 400 mg/dose) for 10 days. To treat pharyngitis and tonsillitis caused by S. pyogenes ORAL SUSPENSION, Adults and adolescents over age 13. 100 mg every 12 hr for 5 to 10 days. Children ages 2 months through 12 years. 5 mg/kg every 12 hr for 5 to 10 days. Maximum: 100 mg/dose.
DOSAGE ADJUSTMENT Dosing interval increased to 24 hr in patients with creatinine clearance less than 30 ml/min/1.73 m2.

Mechanism of Action

Interferes with bacterial cell wall synthesis cefpodoxime proxetil 201 C by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity antacids, H2-receptor antagonists: Reduced bioavailability and blood level of cefpodoxime oral anticholinergics: Delayed peak blood level of cefpodoxime probenecid: Possibly increased and prolonged blood cefpodoxime level

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis, superinfection

Cautions

Use cefpodoxime cautiously in patients who have impaired renal function or are receiving potent diuretics. Also use drug cautiously in patients hypersensitive to penicillin because cross-sensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity test results, as ordered, before giving cefpodoxime.

Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Be aware that an allergic reaction may occur a few days after therapy starts.

PATIENT SAFTY

Urge patient to complete the prescribed course of therapy.

Tell patient to take tablets with food to enhance absorption.

Advise patient to refrigerate oral suspension and discard after 14 days.

Instruct patient to shake oral suspension bottle well before pouring dose and to use a calibrated liquid-measuring device to ensure accurate doses.

Inform patient that yogurt and buttermilk can help maintain intestinal flora and decrease diarrhea.

Warn patient not to take an antacid within 2 hours before or after taking cefpodoxime.

Tell patient to report watery, bloody stools to prescriber immediately, even up to 2 months after drug therapy has ended.

Category

Chemical class: Second-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat secondary bacterial infections in patients with acute bronchitis and acute bacterial exacerbations of acute bronchitis caused by Haemophilus influenzae, Moraxella catarrhalis, and Streptococcus pneumoniae ORAL SUSPENSION, Adults and adolescents. 500 mg every 12 hr for 10 days. To treat uncomplicated skin and softtissue infections caused by Staphylococcus aureus and Streptococcus pyogenes ORAL SUSPENSION, Adults and adolescents.250 mg every 12 hr or 500 mg every 12 to 24 hr for 10 days. Children ages 2 to 12. 20 mg/kg every 24 hr for 10 days. To treat pharyngitis and tonsillitis caused by S. pyogenes cefprozil 202 ORAL SUSPENSION, Adults and adolescents.500 mg every 24 hr for 10 days. Children ages 2 to 12. 7.5 mg/kg every 12 hr for 10 days. To treat otitis media caused by H. influenzae, M. catarrhalis, and S. pneumoniae ORAL SUSPENSION, Children ages 6 months to 12 years. 15 mg/kg every 12 hr for 10 days. To treat acute sinusitis caused by H. influenzae, M. catarrhalis, and S. pneumoniae ORAL SUSPENSION, Adults and adolescents.250 to 500 mg every 12 hr for 10 days. Children ages 6 months to 12 years. 7.5 or 15 mg/kg every 12 hr for 10 days.
DOSAGE ADJUSTMENT Dosage reduced by half and given at usual intervals in patients with creatinine clearance less than 30 ml/ min/1.73 m2.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes the cell membrane rigid and protective. Without it, bacterial cells rupture and die.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity probenecid: Increased blood cefprozil level

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis, superinfection

Cautions

Use cefprozil cautiously in patients who have impaired renal function or a history of GI disease, especially colitis. Also use drug cautiously in patients who are hypersensitive to penicillin because crosssensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.
WARNING Don’t administer oral suspension to patients with phenylketonuria because it contains phenylalanine 28 mg/5 ml.

Monitor BUN and serum creatinine levels to detect early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.

Be aware that an allergic reaction may occur a few days after therapy starts.

Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

PATIENT SAFTY

Urge patient to complete the prescribed course of therapy.

Tell patient to refrigerate oral suspension and discard after 14 days.

Instruct patient to shake oral suspension well before pouring and to use a calibrated measuring device to ensure accurate doses.

Inform patient that yogurt and buttermilk can help maintain intestinal flora and decrease diarrhea.

Tell patient to report watery, bloody stools to prescriber immediately, even up to 2 months after drug therapy has ended.

Category

Chemical class: Third-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

ceftazidime 203 C

Indications

To treat infections caused by gramnegative organisms (including Acinetobacter, Citrobacter, Enterobacter, Escherichia coli, Haemophilus influenzae, Klebsiella, Neisseria, Proteus mirabilis, Proteus vulgaris, Pseudomonas aeruginosa, Salmonella, Serratia, and Shigella), gram-positive organisms (including Streptococcus agalactiae, Streptococcus pneumoniae, and Streptococcus pyogenes [group B streptococci]), as well as Staphylococcus aureus (penicillinaseand non– penicillinase-producing strains)
IV:,
I.M.INJECTION Adults and children age 12 and over.1 g every 8 to 12 hr.
IV: Children ages 1 month to 12 years. 30 to 50 mg/kg every 8 hr. Neonates up to age 1 month.30 mg/kg every 12 hr. Maximum: 6 g daily. To treat uncomplicated UTI
IV:,
I.M.INJECTION Adults and children age 12 and over. 250 mg every 12 hr. To treat complicated UTI
IV:,
I.M.INJECTION Adults and children age 12 and over. 500 mg every 8 to 12 hr. To treat uncomplicated pneumonia and mild skin and soft-tissue infections
IV:,
I.M.INJECTION Adults and children age 12 and over. 0.5 to 1 g every 8 hr. To treat bone and joint infections
IV: Adults and children age 12 and over.2 g every 12 hr. To treat serious gynecologic and intraabdominal infections, meningitis, and life-threatening infections, especially in immunocompromised patients
IV: Adults and children age 12 and over. 2 g every 8 hr. To treat pseudomonal lung infection in patients with cystic fibrosis and normal renal function

IV

Adults and children age 1 month and over. 30 to 50 mg/kg every 8 hr. Maximum: 6 g daily. Neonates up to age 1 month.30 mg/kg every 12 hr.
DOSAGE ADJUSTMENT Dosage reduced to 1 g every 12 hr if creatinine clearance is 31 to 50 ml/min/1.73 m2; to 1 g every 24 hr if 16 to 30 ml/min/1.73 m2; to 0.5 g every 24 hr if 6 to 15 ml/min/1.73 m2; and to 0.5 g every 48 hr if less than 6 ml/min/ 1.73 m2.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the cross-linking of peptidoglycan strands. Peptidoglycan makes the cell membrane rigid and protective. Without it, bacterial cells rupture and die.

Incompatibilities

Don’t mix ceftazidime with aminoglycosides to prevent mutual inactivation. Vancomycin is physically incompatible with ceftazidime (precipitate may form); flush I.V. line between these if given through same tubing. Avoid mixing ceftazidime with other , including pentamidine isethionate.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity oral combined estrogen-progesterone contraceptives: Decreased effectiveness of oral contraceptive

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome ceftazidime 204
Other: Anaphylaxis; injection site pain, redness, and swelling; superinfection

Cautions

Use ceftazidime cautiously in patients hypersensitive to penicillin because crosssensitivity occurs in about 10% of such patients. Watch for allergic reactions a few days after therapy starts.

Use cautiously in patients with a history of GI disease, particularly colitis, because risk of pseudomembranous colitis is increased.

Ceftazidime l-arginine (Ceptaz) is not recommended for children under age 12.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

Protect ceftazidime powder and reconstituted drug from heat and light; both tend to darken during storage.

If pharmacy delivers frozen solution, thaw it at room temperature, not in water bath or microwave. Store thawed solution for up to 12 hours at room temperature or 7 days in refrigerator; don’t refreeze.
WARNING When preparing drug for neonates or immature infants, don’t use diluents containing benzyl alcohol because they are linked to a fatal toxic syndrome.

For I.V. bolus, reconstitute 1 to 2 g with 10 ml sterile water for injection, D5W, or sodium chloride for injection. Shake to dissolve. Administer I.V. injection slowly over 3 to 5 minutes through tubing of a flowing compatible I.V. fluid.

For intermittent infusion, further dilute in 50 to 100 ml D5W or normal saline solution. Avoid using sodium bicarbonate injection as a diluent because drug is least stable in it. During ceftazidime administration, temporarily stop other solutions being given at the same I.V. site.

For I.M. use, reconstitute each gram with 3 ml sterile water for injection or bacteriostatic water for injection.

Give I.M. injection deep into large muscle mass, such as gluteus maximus.

Rotate I.V. sites every 72 hours. Assess for phlebitis and extravasation.

Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Monitor CBC, hematocrit, and serum AST, ALT, bilirubin, LD, and alkaline phosphatase levels during long-term therapy.

Monitor PT, as ordered, in at-risk patients, such as those with renal or hepatic impairment or poor nutritional state and those receiving anticoagulant or prolonged antibiotic therapy. Notify prescriber if PT decreases, and expect to give vitamin K.

Assess patient for perineal itching, fever, malaise, redness, swelling, rash, and change in cough or sputum; they may indicate a superinfection.

Watch for pharyngitis, ecchymosis, bleeding, and arthralgia (possible blood dyscrasia). Monitor PT and bleeding time.

PATIENT SAFTY

Tell patient to take ceftazidine exactly as prescribed.

Tell patient to immediately report evidence of blood dyscrasia or superinfection to prescriber.

Urge patient to report watery, bloody stools to prescriber immediately, even up to 2 months after drug therapy has ended.

Category

Chemical class: Third-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat acute bacterial exacerbations of chronic bronchitis caused by Haemophilus influenzae, Moraxella catarrhalis, or Streptococcus pneumoniae; pharyngitis and tonsillitis caused by Streptococcus pyogenes; and acute bacterial otitis media caused by H. influenzae, M. catarrhalis, or S. pneumoniae , ORAL SUSPENSION Adults and children age 12 and over. 400 mg daily for 10 days. To treat pharyngitis and tonsillitis caused by S. pyogenes and acute bacterial otitis media caused by H. influenzae, M. catarrhalis, or S. pneumoniae ORAL SUSPENSION Children under age 12. 9 mg/kg daily for 10 days. Maximum: 400 mg daily.
DOSAGE ADJUSTMENT Dosage reduced to 4.5 mg/kg or 200 mg every 24 hr if creatinine clearance is 30 to 49 ml/min/1.73 m2; ceftibuten 205 C to 2.25 mg/kg or 100 mg every 24 hr if it’s 5 to 29 ml/min/1.73 m2.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the cross-linking of peptidoglycan strands. Peptidoglycan makes the cell membrane rigid and protective. Without it, bacterial cells rupture and die.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity

Side Efect

CNS: Aphasia, chills, fever, headache, psychosis, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, jaundice, melena, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, serum sickness, superinfection

Cautions

Use ceftibuten cautiously in patients hypersensitive to penicillins because crosssensitivity occurs in up to 10% of such patients.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

Refrigerate oral suspension; shake well before using. Discard after 14 days.

Monitor BUN and serum creatinine levels to detect early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.

Be aware that an allergic reaction may occur a few days after therapy starts.

Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Assess patient for perineal itching, fever, malaise, redness, swelling, rash, and change in cough or sputum; they may indicate a superinfection.

Assess for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

PATIENT SAFTY

Urge patient to complete the drug therapy as prescribed.

Instruct patient to take drug on an empty stomach at least 2 hours before or 1 hour after meals.

Inform patient that unflavored oral suspension has a bitter taste. Suggest having a flavor added when prescription is filled.

Advise patient that yogurt and buttermilk can help maintain intestinal flora and decrease diarrhea during therapy.

Tell patient to immediately report hypersensitivity reactions, severe diarrhea, and evidence of blood dyscrasia or superinfection.

Category

Chemical class: Third-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat mild to moderate infections of the lower respiratory tract, skin, soft tissue, bones, and joints; septicemia; meningitis; and intra-abdominal infections caused by anaerobes (such as Bacteroides species, Peptococcus, and Peptostreptococcus), gram-negative organisms (including Escherichia coli, Haemophilus influenzae, Klebsiella, and Proteus mirabilis), and grampositive organisms (including Enterobacter species, Serratia species, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus agalactiae, Streptococcus pneumoniae, and Streptococcus pyogenes) ceftizoxime sodium 206
IV:, I.V.OR
I.M.INJECTION Adults and children age 12 and over.1 to 2 g every 8 to 12 hr. To treat severe or refractory infections of the type listed above
IV: OR INJECTION Adults and children age 12 and over.1 g every 8 hr or 2 g every 8 to 12 hr. To treat life-threatening infections of the type listed above
IV: OR INJECTION Adults and children age 12 and over.3 to 4 g every 8 hr or, if required, up to 2 g every 4 hr. To treat bacterial infections in children
IV:, I.V.OR
I.M.INJECTION Children age 6 months and over. 50 mg/kg every 6 to 8 hr. To treat uncomplicated UTI
IV:, I.V.OR
I.M.INJECTION
Adults.500 mg every 12 hr. To treat pelvic inflammatory disease
IV: OR INJECTION
Adults. 2 g every 8 hr. To treat uncomplicated gonococcal infections
I.M.INJECTION
Adults.1 g as a single dose.
DOSAGE ADJUSTMENT Dosage reduced to 0.5 g every 8 hr for less severe infections and 0.75 to 1.5 g every 8 hr for life-threatening infections if creatinine clearance is 50 to 79 ml/min/1.73 m2; to 0.25 to 0.5 g every 12 hr for less severe infections and 0.5 to 1 g every 12 hr for life-threatening infections if creatinine clearance is 5 to 49 ml/min/1.73 m2; and to 0.5 g every 48 hr or 0.25 g every 24 hr for less severe infections and 0.5 to 1 g every 48 hr or 0.5 g every 24 hr for life-threatening infections if creatinine clearance is 4 ml/min/1.73 m2or less.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes the cell membrane rigid and protective. Without it, bacterial cells rupture and die.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis; injection site pain, redness, and swelling; superinfection

Cautions

Use ceftizoxime cautiously in patients hypersensitive to penicillin because crosssensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

For I.V. administration, reconstitute with sterile water for injection as follows: for 500-mg vial, add 5 ml; for 1-g vial, add 10 ml; and for 2-g vial, add 20 ml. Shake well. Dilute reconstituted solution further with 50 to 100 ml of a compatible solution, such as normal saline solution or D5W, before administration. Give I.V. injection slowly over 3 to 5 minutes through tubing of a flowing compatible I.V. fluid.

For I.M. administration, reconstitute with sterile water for injection as follows: for 500-mg vial, add 1.5 ml; for 1-g vial, add 3 ml; and for 2-g vial, add 6 ml. Shake well. Divide 2-g doses and administer in different sites. Inject deep in large muscle mass, such as the gluteus maximus.

Reconstituted drug may be stored 24 hours at room temperature or 96 hours if refrigerated.

Assess I.V. site for extravasation and ceftizoxime sodium 207 C phlebitis.

Monitor BUN and serum creatinine levels to detect early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.

Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Monitor patient for allergic reactions a few days after therapy starts.

Assess CBC, hematocrit, and serum AST, ALT, bilirubin, LD, and alkaline phosphatase levels during long-term therapy.

Assess patient for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

PATIENT SAFTY

Advise patient to immediately report severe or persistent diarrhea or evidence of blood dyscrasia to prescriber.

Category

Chemical class: Third-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat infections of the lower respiratory tract, skin, soft tissue, urinary tract, bones, and joints; sinusitis; intraabdominal infections; and septicemia caused by anaerobes (including Bacteroides bivius, Bacteroides fragilis, Bacteroides melaninogenicus, and Peptostreptococcus species), gramnegative organisms (including Citrobacter species, Enterobacter aerogenes, Escherichia coli, Haemophilus influenzae, Klebsiella species, Neisseria species, Proteus mirabilis, Proteus vulgaris, Providencia species, Salmonella species, Serratia marcescens, Shigella, and some strains of Pseudomonas aeruginosa), and gram-positive organisms (including Staphylococcus aureus, Streptococcus pneumoniae, and Streptococcus pyogenes)
IV:,
I.M.INJECTION
Adults.1 to 2 g daily or in equally divided doses b.i.d. Maximum: 4 g daily. Children.50 to 75 mg/kg daily in divided doses every 12 hr. Maximum: 2 g daily. To treat meningitis
IV: Children. Initial: 100 mg/kg on first day, then 100 mg/kg daily or in divided doses every 12 hr for 7 to 14 days. Maximum: 4 g daily. To treat acute bacterial otitis media
I.M.INJECTION Children.50 mg/kg as a single dose. Maximum: 1 g. To treat chancroid (Haemophilus ducreyi infection) and uncomplicated gonorrhea
I.M.INJECTION
Adults. 250 mg as a single dose. To treat gonococcal conjunctivitis
I.M.INJECTION
Adults.1 g as a single dose. To treat disseminated gonoccocal infection and pelvic inflammatory disease
IV:,
I.M.INJECTION
Adults. 1 g every 24 hr. To treat gonococcal meningitis and endocarditis
IV:
Adults. 1 to 2 g every 12 hr for 10 to 14 days (meningitis) or for 4 wk or longer (endocarditis). To provide surgical prophylaxis
IV:
Adults.1 g 30 min to 2 hr before surgery.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting cross-linking of peptidoglycan strands. Peptidoglycan makes the cell membrane rigid and protective. Without it, bacterial cells rupture and die.

Incompatibilities

Don’t admix ceftriaxone with pentamidine isethionate, labetalol, or other antibiotics, such as aminoglycosides, because of potential for incompatibility, such as substantial mutual inactivation. Also don’t mix with calcium-containing solutions or products because a ceftriaxone-calcium salt may precipitate in the lungs and kidneys and may be fatal, especially in newborns.

Contraindications

Calcium-containing I.V. solutions; hyperceftriaxone sodium 208 bilirubinemic neonates 28 days old or less if they’re expected to need calcium-containing solutions, including parenteral nutrition; hypersensitivity to ceftriaxone, other cephalosporins, or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity

Side Efect

CNS: Chills, fever, headache, hypertonia, reversible hyperactivity, seizures
CV: Edema
EENT: Glossitis, hearing loss, stomatitis
GI: Abdominal cramps, cholestasis, diarrhea, elevated liver function test results, gallbladder dysfunction, hepatic failure, hepatomegaly, nausea, oral candidiasis, pancreatitis, pseudolithiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, oliguria, renal failure, vaginal candidiasis
HEME: Aplastic anemia, eosinophilia, hemolytic anemia, hemorrhage, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Allergic pneumonitis, dyspnea
SKIN: Allergic dermatitis, ecchymosis, erythema, erythema multiforme, exanthema, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis; drug fever; injection site pain, redness, and swelling; serum sickness; superinfection

Cautions

WARNING Calcium-containing products must not be given I.V. within 48 hours of ceftriaxone, including solutions given through a different I.V. line and at a different site, because a ceftriaxone-calcium salt may precipitate in the lungs and kidneys and could be fatal.

Use ceftriaxone cautiously in patients who are hypersensitive to penicillins because cross-sensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity results, as ordered, before giving drug.

Protect powder from light.

For I.V. use, reconstitute with an appropriate diluent, such as sterile water for injection or sodium chloride for injection, as follows: for 250-mg vial, add 2.4 ml; for 500-mg vial, add 4.8 ml; for 1-g vial, add 9.6 ml; and for 2-g vial, add 19.2 ml to yield 100 mg/ml. For piggyback bottles, reconstitute with 10 ml of diluent indicated above for 1-g bottle and 20 ml for 2-g bottle. After reconstitution, further dilute to 50 to 100 ml with diluent indicated above and infuse over 30 minutes.
WARNING Never give ceftriaxone by I.V. infusion and calcium-containing IV solutions at the same time, including such continuous calcium-containing infusions as parenteral nutrition via Y-site. For patients other than neonates, ceftriaxone and calcium-containing solutions may be given sequentially if infusion lines are thoroughly flushed with a compatible fluid between infusions.

For I.M. administration, reconstitute with an appropriate diluent, such as sterile water for injection or sodium chloride for injection, as follows: for 250-mg vial, add 0.9 ml; for 500-mg vial, add 1.8 ml; for 1-g vial, add 3.6 ml; and for 2-g vial, add 7.2 ml to make a 250-mg/ml concentration. Shake well. Inject deep into large muscle mass, such as the gluteus maximus.

Monitor BUN and serum creatinine levels to detect early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.

Monitor patient for allergic reactions a few days after therapy starts.

Assess CBC, hematocrit, and serum AST, ALT, bilirubin, LD, and alkaline phosphatase levels during long-term therapy. If abnormalities occur, notify prescriber. Drug may need to be discontinued.

Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold cefotaxime and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Monitor patient for evidence of gallbladder disease (abdominal pain, nausea, vomiting) because drug may cause ceftriaxonecalcium salt to deposit in the gallbladder, which may mimic gallstones. Expect drug to be discontinued if gallbladder disorders arise. ceftriaxone sodium 209 C

Assess for perineal itching, fever, malaise, redness, swelling, rash, and change in cough or sputum; they may indicate a superinfection.

Assess for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

PATIENT SAFTY

Tell patient to immediately report evidence of blood dyscrasia or superinfection to prescriber.

Urge patient to report watery, bloody stools to prescriber immediately, even up to 2 months after drug therapy has ended.

Category

Chemical class: Second-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat pharyngitis and tonsillitis ORAL SUSPENSION Children ages 3 months to 12 years. 10 mg/kg daily in equally divided doses b.i.d. for 10 days. Maximum: 500 mg daily. Adults and children age 13 and over. 250 mg b.i.d. for 10 days. Children under age 13 who can swallow tablets. 125 mg b.i.d. for 10 days. To treat acute otitis media ORAL SUSPENSION Children ages 3 months to 12 years. 30 mg/kg daily in equally divided doses b.i.d. for 10 days. Maximum: 1,000 mg daily. Children under age 13 who can swallow tablets. 250 mg b.i.d. for 10 days. To treat impetigo ORAL SUSPENSION Children ages 3 months to 12 years. 30 mg/ kg daily in equally divided doses b.i.d. for 10 days. Maximum: 1,000 mg daily. To treat acute bacterial maxillary sinusitis ORAL SUSPENSION Children ages 3 months to 12 years. 30 mg/ kg daily in equally divided doses b.i.d. for 10 days. Maximum: 1,000 mg daily. Adults and children age 13 and over and children under age 13 who can swallow tablets. 250 mg b.i.d. for 10 days. To treat acute bacterial exacerbations of chronic bronchitis and uncomplicated skin and soft-tissue infections Adults and children age 13 and over. 250 to 500 mg b.i.d. for 10 days.
IV:, I.V.OR
I.M.INJECTION
Adults.750 mg every 8 hr. To treat secondary bacterial infection in patients with acute bronchitis Adults and children age 13 and over. 250 to 500 mg b.i.d. for 5 to 10 days. To treat early Lyme disease Adults and children age 13 and over. 500 mg b.i.d. for 20 days. To treat uncomplicated UTI
Adults.125 to 250 mg b.i.d. for 7 to 10 days.
IV:, I.V.OR
I.M.INJECTION
Adults. 750 mg every 8 hr. To treat uncomplicated gonorrhea
Adults.1 g as a single dose.
I.V.INJECTION
Adults.1.5 g as a single dose divided equally and injected into two different sites; given with oral probenecid 1 g. To treat disseminated gonococcal infection and uncomplicated pneumonia
IV:, I.V.OR
I.M.INJECTION
Adults.750 mg every 8 hr. To treat bone and joint infections
IV:, I.V.OR
I.M.INJECTION
Adults.1.5 g every 8 hr. Children over age 3 months.50 to 150 mg/ kg daily in divided doses every 8 hr. Maximum: Adult dose. To treat bacterial meningitis
IV:
Adults.1.5 to 3 g every 8 hr. Children over age 1 month. 50 to 80 mg/kg every 6 to 8 hr. cefuroxime 210 Neonates up to age 1 month.33.3 to 50 mg/ kg every 8 to 12 hr. To treat moderate infections other than those listed above
IV:, I.V.OR
I.M.INJECTION
Adults. 750 mg every 8 hr for 5 to 10 days.
IV: OR INJECTION Children over age 3 months. 50 mg/kg daily in equally divided doses every 6 to 8 hr. To treat severe or complicated infections other than those listed above
IV: OR INJECTION
Adults. 1.5 g every 8 hr. Children over age 3 months.100 mg/kg daily in equally divided doses every 6 to 8 hr. To treat life-threatening infections other than those listed above
IV: OR INJECTION
Adults.1.5 g every 6 hr. To provide perioperative prophylaxis
IV: OR INJECTION
Adults.1.5 g 30 to 60 min before surgery (at induction of anesthesia for open-heart surgery), and then 0.75 g every 8 hr thereafter (1.5 g every 12 hr for total of 6 g with open-heart surgery).
DOSAGE ADJUSTMENT Parenteral dosage reduced to 0.75 g every 12 hr if creatinine clearance is 10 to 20 ml/min/1.73 m2or to 0.75 g every 24 hr if creatinine clearance less than 10 ml/min/1.73 m2.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes the cell membrane rigid and protective. Without it, bacterial cells rupture and die.

Incompatibilities

Don’t admix parenteral cefuroxime with other antibiotics, such as aminoglycosides, because of potential for incompatibility, such as substantial mutual inactivation. If they’re administered concurrently, don’t mix them in the same I.V. bag or bottle.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity antacids, H2-receptor antagonists, omeprazole: Decreased cefuroxime axetil absorption probenecid: Increased and prolonged blood cefuroxime level

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss, oral candidiasis
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis; injection site edema, pain, and redness; superinfection

Cautions

Use cefuroxime cautiously in patients hypersensitive to penicillin because crosssensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity results, as ordered, before giving drug.

Give oral form with food to decrease GI distress, as needed.

Remember that oral forms—tablets and suspension—aren’t bioequivalent.

For I.V. use, reconstitute using manufacturer’s instructions according to type of preparation available. Solution ranges in color from light yellow to amber.

For I.M. use, add 3 or 3.6 ml sterile water for injection to each 750-mg vial to yield 220 mg/ml.

If using a container of frozen parenteral solution, thaw at room temperature or under refrigeration before administration; make sure all ice crystals have melted. Don’t force thawing by microwaving.

Store reconstituted parenteral drug for up to 24 hours at room temperature or 96 hours in refrigerator. (Thawed solutions may be stable 24 hours at room temperature or 28 days if refrigerated.) Store reconstituted oral suspension in refrigeracefuroxime 211 C tor or at room temperature up to 10 days.

Give I.V. injection over 3 to 5 minutes through tubing of a flowing compatible I.V. fluid.

Monitor I.V. site for extravasation and phlebitis.

Monitor BUN and serum creatinine levels and fluid intake and output to detect signs of nephrotoxicity. Monitor patients with renal impairment closely because they may have greater toxic reactions to cefuroxime.

Monitor patient for allergic reactions continuing up to a few days after therapy starts. Patients with a history of some form of allergy, especially to , are at increased risk for an allergic reaction.

Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis. If it’s suspected, stop drug, as ordered, and provide treatment as prescribed.

Assess patient for pharyngitis, ecchymosis, bleeding, and arthralgia, which may indicate a blood dyscrasia.

Monitor PT and bleeding time, as ordered. Be prepared to administer vitamin K, if ordered, to treat hypothrombinemia.

PATIENT SAFTY

Instruct patient to shake oral suspension well before measuring each dose and to use a calibrated liquid-measuring device.

Advise patient using single-dose packets of oral suspension to empty contents of one packet into a glass and add at least 10 ml (2 tsp) of cold water; apple, grape, or orange juice; or lemonade. Tell him to stir well and consume entire mixture at once.

Inform patient that yogurt and buttermilk help maintain intestinal flora and can decrease diarrhea during therapy.

Instruct patient to report evidence of blood dyscrasia to prescriber immediately.

Urge patient to report watery, bloody stools to prescriber immediately, even up to 2 months after drug therapy has ended.

Category

Chemical class: Diaryl-substituted pyrazole derivative
Therapeutic class: Anti-inflammatory, antirheumatic

Pregnancy category: C

Indications

To relieve signs and symptoms of osteoarthritis
Adults.200 mg daily or 100 mg b.i.d. To relieve signs and symptoms of rheumatoid arthritis
Adults.100 to 200 mg b.i.d. To relieve signs and symptoms of juvenile rheumatoid arthritis Children age 2 and older weighing 10 to 25 kg (22 to 55 lb). 50 mg b.i.d. Children age 2 and older weighing more than 25 kg. 100 mg b.i.d. To relieve pain from ankylosing spondylitis
Adults. 200 mg daily or 100 mg b.i.d. Dosage increased to 400 mg daily or 200 mg b.i.d. after 6 weeks if needed. As adjunct to reduce adenomatous colorectal polyps in patients with familial adenomatous polyposis
Adults.400 mg b.i.d. To manage acute pain, to treat primary dysmenorrhea
Adults.400 mg, followed by 200 mg if needed, on 1st day. On subsequent days, 200 mg b.i.d. as needed.
DOSAGE ADJUSTMENT Daily dosage reduced for patients with hepatic impairment. For those weighing less than 50 kg (110 lb), expect to start with lowest recommended dose. For patients who are poor CYP2C9 metabolizers, starting dosage should be half the lowest recommended dose.

Mechanism of Action

Selectively inhibits the enzymatic activity of cyclooxygenase-2 (COX-2), the enzyme needed to convert arachidonic acid to prostaglandin. Prostaglandins are responsible for mediating the inflammatory response and causing local vasodilation, swelling, and pain. Prostaglandins also play a role in peripheral pain transmission to the spinal cord. By inhibiting COX-2 activity celecoxib 212 and prostaglandin production, this NSAID reduces inflammatory symptoms and relieves pain. Celecoxib’s mechanism of action in reducing the number of colorectal polyps is unknown.

Contraindications

Allergic reaction (such as anaphylaxis or angioedema) to aspirin, other NSAIDs, or sulfonamide derivatives or history of aspirin-induced nasal polyps with bronchospasm; hypersensitivity to celecoxib or its components; treatment of perioperative pain after coronary artery bypass graft surgery

Interactions

ACE inhibitors, angiotensin II receptor antagonists: Decreased antihypertensive effect of ACE inhibitors and angiotensin II receptor antagonists, increased risk of renal failure aspirin: Increased risk of GI ulceration and other GI complications fluconazole: Increased blood celecoxib level furosemide, thiazide diuretics: Reduced diuretic effects of these , increased risk of renal failure lithium: Possibly elevated blood lithium level
warfarin: Possibly increased PT and risk of bleeding

Side Efect

CNS: Asceptic meningitis, cerebral hemorrhage, depression, dizziness, fever, headache, insomnia, ischemic stroke, stroke, suicidal ideation, syncope, transient ischemic attacks, vertigo
CV: Aortic valve incompetence, chest pain, congestive heart failure, deep vein thrombosis, fluid retention, hypertension, MI, palpitations, peripheral edema or gangrene, sinus bradycardia, tachycardia, thrombosis, unstable angina, vasculitis, ventricular fibrillation, ventricular hypertrophy
EENT: Conjunctival hemorrhage, deafness, labyrinthitis, nasopharyngitis, pharyngitis, rhinitis, sinusitis, vitreous floaters
ENDO: Hyperglycemia, hypoglycemia
GI: Abdominal pain, diarrhea, elevated liver function test results, esophageal perforation, flatulence, GI bleeding or ulceration, hepatic failure, ileus, indigestion, jaundice, nausea, pancreatitis, perforation of stomach or intestine, vomiting
GU: Acute renal failure, interstitial nephritis, ovarian cyst, proteinuria, UTI, urinary incontinence
HEME: Agranulocytosis, aplastic anemia, decreased hematocrit and hemoglobin, leukopenia, pancytopenia, prolonged APTT, thrombocytopenia
MS: Arthralgia, back pain, elevated serum CK level, epicondylitis, tendon rupture
RESP: Bronchospasm, cough, dyspnea, pneumonia, pulmonary embolism, upper respiratory tract infection
SKIN: Erythema multiforme, exfoliative dermatitis, phototoxicity, rash, StevensJohnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, hyperkalemia, hypernatremia, hyponatremia, sepsis

Cautions

Use celecoxib with extreme caution in patients who have a history of ulcer disease or GI bleeding because NSAIDs, such as celecoxib, increase the risk of GI bleeding and ulceration. In these patients, drug should be used for shortest time possible.

Be aware that serious GI tract ulceration and bleeding, as well as perforation of stomach or intestine, can occur without
WARNING or symptoms. Elderly patients are at greatest risk. To minimize risk, give celecoxib with food. If patient develops GI distress, withhold celecoxib and notify prescriber immediately.

Use celecoxib cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy because drug can start or worsen hypertension.

Use celecoxib cautiously in children with systemic onset juvenile rheumatoid arthritis because serious

Side Efect

can occur, including disseminated intravascular coagulation.

Use celecoxib cautiously in patients known to be poor CYP2C9 metabolizers based on history or experience with other CYP2C9 substrates, such as warfarin or phenytoin. Dosage should start at half the lowest recommended amount. For patients with juvenile rheumatoid arthritis who are also poor CYP2C9 metabolizers, alternative management should be considered.
WARNING Monitor patient closely for celecoxib 213 C thrombotic events, including MI and stroke, because use (especially long-term use) of NSAIDs such as celecoxib increases the risk.
WARNING In patient who has bone marrow suppression or is receiving antineoplastic therapy, monitor laboratory results (including WBC) and assess for infection because celecoxib’ anti-inflammatory and antipyretic actions may mask signs and symptoms, such as fever and pain.

Monitor patient—especially if elderly or receiving long-term celecoxib therapy— for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results because, in rare cases, elevation may progress to severe hepatic reaction, including fatal hepatitis, hepatic necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in elderly patients; patients taking diuretics, ACE inhibitors, or angiotensin II receptor antagonists; and patients with heart failure, impaired renal function, or hepatic dysfunction because drug may cause renal failure.

Monitor CBC for decreased hemoglobin level and hematocrit because drug may worsen anemia.

Assess patient’s skin regularly for signs of rash or other hypersensitivity reaction because celecoxib is a sulfur drug and may cause serious skin reactions without warning, even in patients with no history of sensivitity to sulfur. At first sign of reaction, stop drug and notify prescriber.

Avoid using celecoxib with a non-aspirin NSAID, regardless of the dose, because celecoxib reduces inflammation and fever, which may mask signs of infection.

PATIENT SAFTY

Instruct patient to swallow celecoxib capsules whole with a full glass of water and with food or milk to prevent stomach upset.

Tell patient to take celecoxib exactly as prescribed and not to increase dosage or take drug longer than prescribed because serious

Side Efect

can occur.

Advise patient to notify prescriber if pain continues or is poorly controlled.

Explain that celecoxib may increase the risk of serious adverse CV events; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, slurred speech, and weakness.

Tell patient that celecoxib may increase the risk of serious adverse GI reactions. Stress the need to seek immediate medical attention if signs or symptoms develop, such as epigastric or abdominal pain, indigestion, black or tarry stools, and vomiting blood or material that resembles coffee grounds.

Alert patient that celecoxib may cause serious skin reactions. Advise immediate medical attention if signs or symptoms develop, such as rash, blisters, fever, itching, or other evidence of hypersensitivity.

Urge patient to avoid smoking and alcohol consumption during celecoxib therapy because they may increase the risk of adverse GI reactions.

Category

Chemical class: First-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat streptococcal tonsillitis, pharyngitis, and skin and soft-tissue infections , ORAL SUSPENSION, Adults and adolescents age 15 and over. 500 mg every 12 hr. Maximum: 4 g daily. Children and adolescents ages 2 to 15. 25 to 50 mg/kg daily divided into two equal doses and given every 12 hr. If infection is severe, dose may be doubled. cephalexin 214 To treat mild to moderate respiratory tract, skin, soft-tissue, bone, and GU infections caused by susceptible organisms other than streptococci , ORAL SUSPENSION,
Adults.250 mg every 6 hr. ORAL SUSPENSION Children.25 to 50 mg/kg daily in equally divided doses b.i.d. or q.i.d. To treat severe respiratory tract, skin, soft-tissue, bone, and GU infections , ORAL SUSPENSION,
Adults. 0.5 to 1 g every 6 hr. Maximum: 4 g daily. Children.50 to 100 mg/kg daily in equally divided doses q.i.d. To treat otitis media ORAL SUSPENSION Children. 75 to 100 mg/kg daily in equally divided doses q.i.d. To treat uncomplicated cystitis , ORAL SUSPENSION, Adults and adolescents age 15 and over. 500 mg every 12 hr.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity probenecid: Increased and prolonged blood cephalexin level

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis, superinfection

Cautions

Use cephalexin cautiously in patients hypersensitive to penicillin because crosssensitivity occurs in about 10% of them.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

Monitor patient’s BUN and serum creatinine levels to detect early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.

Monitor for allergic reactions a few days after therapy starts.

Assess CBC, hematocrit, and serum AST, ALT, bilirubin, LD, and alkaline phosphatase levels during long-term therapy.

Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold cefotaxime and treat cephalexin 215 C Bacterial cell interior Bacterial cell exterior Peptidoglycan strand Cephalexin

Mechanism of Action

Like all cephalosporins, cephalexin interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes the cell membrane rigid and protective. Without it, bacterial cells rupture and die. This mechanism of action is most effective against bacteria that divide rapidly, including many gram-positive and gram-negative bacteria. with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Assess patient for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

PATIENT SAFTY

Advise patient to complete prescribed course of therapy.

Instruct patient to shake oral suspension well before measuring each dose and to use a calibrated liquid-measuring device to ensure an accurate dose.

Tell patient that yogurt and buttermilk can help maintain intestinal flora and decrease diarrhea during therapy.

Urge patient to immediately report watery, bloody stools to prescriber, even if they occur up to 2 months after cephalexin therapy has ended.

Category

Chemical class: First-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat respiratory tract infection, skin and soft-tissue infections, UTI, septicemia, endocarditis, and osteomyelitis caused by gram-negative organisms (including Escherichia coli, Haemophilus influenzae, Klebsiella species, and Proteus mirabilis) and grampositive organisms (including group A beta-hemolytic streptococci, Streptococcus pneumoniae, and staphylococci, including coagulase-positive, coagulasenegative, and penicillinase-producing strains but not methicillin-resistant Staphylococcus aureus)
IV:, I.V.OR
I.M.INJECTION
Adults.0.5 to 1 g every 4 to 6 hr. Maximum: 12 g daily. For serious infections, higher doses are given by I.V. route. Children over age 3 months. 40 to 80 mg/ kg daily divided into four equal doses and given every 6 hr. Maximum: 12 g daily. To provide surgical prophylaxis
IV:, I.V.OR
I.M.INJECTION
Adults.1 to 2 g 30 to 60 min before surgery, 1 to 2 g during long procedure, and 1 to 2 g every 6 hr after surgery for 24 hr.
DOSAGE ADJUSTMENT For open-heart surgery or prosthetic arthroplasty, prophylaxis continued 3 to 5 days after procedure, if needed.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes the cell membrane rigid and protective. Without it, bacterial cells rupture and die.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity probenecid: Increased and prolonged blood cephapirin level

Side Efect

CNS: Chills, fever, headache, seizures
CV: Edema
EENT: Hearing loss
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis; injection site pain, redness, and swelling; superinfection

Cautions

Use cephapirin cautiously in patients hypersensitive to penicillins because crosssensitivity has occurred in about 10% of such patients.

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

For I.V. injection, reconstitute 1 g with 10 ml or more of appropriate diluent, such cephapirin sodium 216 as sterile water for injection. Administer I.V. injection slowly over 3 to 5 minutes through tubing of a flowing compatible I.V. fluid.

For I.V. infusion, dilute further in 50 ml of D5W or normal saline solution and infuse over 15 to 30 minutes. Stop primary I.V. solution during cephapirin delivery.

For I.M. injection, reconstitute 1-g vial with 2 ml sterile water for injection or bacteriostatic water for injection. Inject deep into large muscle mass, such as the gluteus maximus.

Store reconstituted drug up to 24 hours at room temperature or 10 days refrigerated.

Don’t give cloudy solution.

Assess I.V. site for extravasation and phlebitis.

Monitor BUN and serum creatinine levels to detect early signs of nephrotoxicity. Also, monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.

Monitor patient for allergic reactions a few days after therapy starts.

Assess CBC, hematocrit, and serum AST, ALT, bilirubin, LD, and alkaline phosphatase levels during long-term therapy.

Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.

Assess patient for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

Assess patient for furry tongue, perineal itching, and loose, foul-smelling stool; they may indicate superinfection.

PATIENT SAFTY

Instruct patient to immediately report severe diarrhea or evidence of blood dyscrasia or superinfection to prescriber.

Category

Chemical class: First-generation cephalosporin, 7-aminocephalosporanic acid
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat respiratory tract infections (other than lobar pneumonia) and skin and soft-tissue infections , ORAL SUSPENSION
Adults.250 mg every 6 hr or 500 mg every 12 hr. Maximum: 4 g daily. ORAL SUSPENSION Children age 9 months and over.25 to 50 mg/kg daily in equally divided doses every 6 or 12 hr. Maximum: 4 g daily. To treat lobar pneumonia , ORAL SUSPENSION
Adults. 0.5 g every 6 hr or 1 g every 12 hr. Maximum: 4 g daily. ORAL SUSPENSION Children age 9 months and over.25 to 50 mg/kg daily in equally divided doses every 6 or 12 hr. Maximum: 4 g daily. To treat uncomplicated UTI , ORAL SUSPENSION
Adults.500 mg every 12 hr. For more serious infections, 500 mg every 6 hr or 1,000 mg every 12 hr. Maximum: 4 g daily. To treat otitis media caused by Haemophilus influenzae ORAL SUSPENSION Children.75 to 100 mg/kg daily in equally divided doses every 6 to 12 hr. Maximum: 4 g daily.
DOSAGE ADJUSTMENT Dosage reduced to 500 mg every 6 hr if creatinine clearance exceeds 20 ml/min/1.73 m2; 250 mg every 6 hr if clearance is 5 to 20 ml/min/1.73 m2; and 250 mg every 12 hr if clearance is less than 5 ml/min/1.73 m2.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes the cell membrane rigid and protective. Without it, bacterial cells rupture and die.

Contraindications

Hypersensitivity to cephalosporins or their components

Interactions

aminoglycosides, loop diuretics: Increased risk of nephrotoxicity probenecid: Increased and prolonged blood cephradine level

Side Efect

CNS: Chills, fever, headache, seizures cephradine 217 C
CV: Edema
EENT: Hearing loss, oral candidiasis
GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
MS: Arthralgia
RESP: Dyspnea
SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
Other: Anaphylaxis, superinfection

Cautions

If possible, obtain culture and sensitivity test results, as ordered, before giving drug.

Monitor patients hypersensitive to penicillin for evidence of hypersensitivity reaction because cross-sensitivity has occurred in about 10% of such patients.

Store oral suspension for 7 days at room temperature or for 14 days if refrigerated.

Monitor BUN and serum creatinine levels to detect early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.

Monitor patient for allergic reactions a few days after therapy starts. If hypersensitivity develops, be prepared to stop drug and administer antihistamines, corticosteroids, and vasopressors, as ordered. Also prepare to administer oxygen, maintain an open airway, and assist with endotracheal intubation, as appropriate.

Assess CBC, hematocrit, and serum AST, ALT, bilirubin, LD, and alkaline phosphatase levels during long-term therapy.

Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis. Obtain a stool specimen to test for Clostridium difficile. Keep in mind that this serious adverse reaction can occur during therapy or up to several weeks after therapy ends. Also avoid giving antiperistaltic antidiarrheals, such as atropine and diphenoxylate or loperamide, because they may delay elimination of toxins from the bowel and damage the colon from toxin retention. Mild cases may respond after cephradine is discontinued. For moderate or severe cases, be prepared to administer fluids, electrolytes, and protein replacement as ordered.

If patient has a history of GI disease, especially ulcerative colitis, regional enteritis, or antibiotic-associated colitis, assess him often for diarrhea because he is at risk for pseudomembranous colitis.

Assess patient for pharyngitis, ecchymosis, bleeding, and arthralgia; these may indicate a blood dyscrasia.

If patient has a seizure, notify prescriber immediately and expect to discontinue drug. Institute seizure precautions according to facility policy.

PATIENT SAFTY

If patient develops GI distress, advise him to take cephradine with food.

Advise patient to complete prescribed course of therapy.

Urge patient to avoid missing doses and to take the drug at evenly spaced intervals. If patient misses a dose, instruct him to take it as soon as possible unless it’s almost time for the next dose. Emphasize that he shouldn’t double the dose.

Tell patient that yogurt and buttermilk help maintain intestinal flora and can decrease diarrhea during therapy.

Instruct patient to immediately report to prescriber severe diarrhea or evidence of blood dyscrasia or superinfection. Warn patient not to take any OTC antidiarrheals before consulting prescriber.

Tell patient to notify prescriber if symptoms don’t improve within a few days.

Category

Chemical class: Recombinant, humanized antibody Fab fragment
Therapeutic class: Disease modifying antiinflammatory

Pregnancy category: B

Indications

To reduce signs and symptoms of Crohn’s disease and maintain clinical response in patients with moderately to severely active disease who have had an certolizumab pegol 218 inadequate response to conventional therapy SUBCUTANEOUS INJECTION
Adults. Initial: 400 mg (given as two 200mg injections) and repeated at wk 2 and 4. Maintenance: 400 mg (given as two 200-mg injections) every 4 wk if clinical response occurs. To treat moderate to severe active rheumatoid arthritis SUBCUTANEOUS INJECTION
Adults.Initial: 400 mg (given as two 200mg injections) and repeated at wk 2 and 4. Maintenance: 200 mg every other wk or 400 mg (given as two 200-mg injections) every 4 wk if clinical response occurs. Route Onset Peak Duration SubQ Unknown 54–171 hr Unknown

Mechanism of Action

Binds to human tumor necrosis factor (TNF) alpha, inhibiting it. TNF alpha stimulates production of inflammatory mediators, including interleukin-1, prostaglandins, platelet activating factor, and nitric oxide. TNF alpha level is increased in patients with Crohn’s disease. Inhibition of TNF alpha causes C-reactive protein level to decline in patients with Crohn’s disease, and the disease improves.

Contraindications

Active infection, hypersensitivity to cetolizu-mab or its components, I.V. administration

Interactions

anakinra: Possibly increased risk of serious infection and neutropenia immunosuppressants: Possibly increased risk of infection live-virus vaccines: Increased risk of adverse vaccine effects

Side Efect

CNS: Anxiety, bipolar disorder, dizziness, fever, malaise, suicidal ideation, syncope
CV: Angina, arrhythmias, heart failure, hypertension, hypotension, MI, pericardial effusion, pericarditis, peripheral edema, vasculitis
EENT: Optic neuritis, retinal hemorrhage, uveitis
ENDO: Hot flashes
GI: Abdominal pain, diarrhea, elevated liver enzymes, hepatitis, intestinal obstruction
GU: Menstrual dysfunction, nephrotic syndrome, pyelonephritis, renal failure, UTI
HEME: Anemia, leukopenia, lyphadenopathy, pancytopenia, thrombophilia
MS: Arthralgia, extremity pain
RESP: Dyspnea, pneumonia, upper respiratory infection
SKIN: Allergic dermatitis, alopecia, erythema multiforme, erythema nodosum, new or worsening psoriasis, rash, Stevens-Johnson sydrome, toxic epidermal necrolysis
Other: Angioedema; bacterial and viral infections; injection site reactions (redness, pain); leukemia, lymphomas, and other malignancies; lupus-like syndrome; serum sickness; tuberculosis

Cautions

Use certolizumab cautiously in patients with recurrent or increased risk of infection, patients who live in regions where tuberculosis and histoplasmosis are endemic, and patients with a history of CNS demyelinating disorders because any of these disorders can occur, rarely, during certolizumab therapy.

Use cautiously in patients who are chronic carriers of hepatitis B virus because drug may reactivate the virus. Assess patient for evidence of hepatitis B viral infection before starting and periodically throughout certolizumab therapy. If HBV reactivation occurs, notify prescriber, stop drug, and start appropriate therapy, as ordered.
WARNING If patient has evidence of an active infection when drug is prescribed, therapy shouldn’t begin until infection has been treated. Monitor all patients for infection during therapy, especially those receiving immunosuppressants. If serious infection develops, expect prescriber to stop drug.

Make sure patient has a tuberculin skin test before therapy starts. If skin test is positive, treatment of latent tuberculosis must start before certolizumab is given, as prescribed.

Reconstitute two 200-mg certolizumab vials for each dose after drug has reached room temperature. Inject 1 ml sterile water for injection using a 20G needle into each vial. Gently swirl each vial without certolizumab pegol 219 C shaking. Then leave vials undisturbed for up to 30 minutes to allow time for powder to completely dissolve. Do not leave at room temperature, once reconstituted, for more than 2 hours before administration. If administration will be delayed, reconstituted drug can be refrigerated up to 24 hours. Do not let drug freeze.

Administer drug only when solution has reached room temperature. Using a 20G needle, withdraw drug from vial using a separate syringe and needle for each vial. Switch to a 23G needle and administer subcutaneously into two separate areas on patient’s abdomen or thigh.
WARNING Stop drug immediately and notify prescriber if patient has an allergic reaction. Expect to provide supportive care.

Monitor patient closely for evidence of congestive heart failure (sudden, unexplained weight gain; dyspnea; crackles; anxiety), and notify prescriber if they occur.

Monitor patient’s CBC, as ordered, because certolizumab may have adverse hematologic effects. Notify prescriber about persistent fever, bruising, bleeding, or pallor.

Certolizumab is a TNF inhibitor. Although rare, malignancies (especially lymphomas and leukemias) have been reported in patients receiving these , including children. Patients with rheumatoid arthritis, especially those with very active disease, are at greatest risk. Monitor them closely.

PATIENT SAFTY

Review signs and symptoms of allergic reaction (rash, swollen face, trouble breathing), and tell patient to seek emergency care immediately if these occur.

Inform patient that injection site reactions such as redness or pain may occur and usually are mild and transient. Instruct him to apply a towel soaked in cold water to the site if it hurts. Tell patient to call prescriber if reaction persists or worsens.

Inform patient that tuberculosis may occur during theray. Instruct him to report persistent cough, wasting or weight loss, and low-grade fever to prescriber.

Tell patient to report evidence of infections and bleeding disorders to prescriber; drug may need to be stopped. Advise patient to avoid people with infections and to comply with all prescribed tests.

Inform patient that certain kinds of cancer, especially lymphomas and leukemias, are more likely in patients taking certolizumab but still rare. Stress need to keep follow-up visits and report unusual or sudden signs or symptoms.

Caution against receiving live-virus vaccines while taking certolizumab; doing so may adversely effect the immune system.

Instruct patient to report lupus-like signs and symptoms that, although rare, may occur during therapy, such as chest pain that doesn’t go away, shortness of breath, joint pain, or rash on cheeks or arms that’s sensitive to the sun. Explain that drug may need to be discontinued if these occur.

Advise patient to inform all health care providers about certolizumab use and to inform prescriber about any OTC medications, herbal remedies, and vitamin and mineral supplements being taken.

Category

Chemical class: Quinuclidine derivative of acetylcholine
Therapeutic class: Cholinergic enhancer, dry mouth reliever

Pregnancy category: C

Indications

To treat dry mouth associated with Sjögren’s syndrome
Adults.30 mg t.i.d. Maximum: 90 mg daily.

Mechanism of Action

As a cholinergic agonist, binds to and activates muscarinic receptors of the parasympathetic nervous system and increases secretions of the exocrine glands, such as salivary glands.

Contraindications

Acute iritis, angle-closure glaucoma, hypersensitivity to cevimeline or its components, uncontrolled asthma cevimeline hydrochloride 220 C

Interactions

amiodarone, cimetidine, clarithromycin, diltiazem, erythromycin, fluconazole, haloperidol, itraconazole, ketoconazole, metoclopramide, mibefradil, nefazodone, propafenone, quinidine, ritonavir, selective serotonin reuptake inhibitors, thioridazine, tricyclic antidepressants, troleandomycin, verapamil: Possibly inhibited metabolism and increased blood level of cevimeline anticholinergics: Decreased effectiveness of anticholinergics antimuscarinics: Altered effects of antimuscarinics and decreased therapeutic action of cevimeline
beta blockers: Possibly cardiac conduction disturbances parasympathomimetics: Additive effects of either drug

Side Efect

CNS: Depression, fatigue, fever, hypoesthesia, insomnia, migraine headache, tremor
CV: Edema, palpitations
EENT: Abnormal vision, conjunctivitis, dry mouth, earache, epistaxis, excessive salivation, eye pain, rhinitis, salivary gland pain
GI: Abdominal pain, anorexia, cholecystitis, constipation, eructation, heartburn, hiccups, nausea, vomiting
HEME: Anemia
MS: Arthralgia, leg cramps, myalgia
RESP: Cough, dyspnea
SKIN: Diaphoresis, pruritus
Other: Flulike symptoms, hot flashes

Cautions

Give cevimeline on an empty stomach because food may decrease rate and extent of absorption, delaying peak concentration.

Assess patient with a pulmonary disorder for wheezing and increased respiratory secretions because drug may cause increased bronchiolar smooth-muscle contractions, airway resistance, and respiratory secretions.

Monitor patient with known or suspected gallbladder disease for abdominal pain and other
WARNINGs of biliary obstruction, cholecystitis, or cholangitis; each of these conditions may be precipitated by cevimeline.

PATIENT SAFTY

Instruct patient to take cevimeline on an empty stomach.

Inform patient that cevimeline may cause vision changes; advise him to avoid driving at night or performing hazardous activities until drug’s adverse effects are known.

Urge patient to drink plenty of fluids during hot weather and while exercising because drug may cause excessive sweating and dehydration.

Category

Chemical class: Chloral derivative
Therapeutic class: Sedative-hypnotic

Pregnancy category: C

Controlled substance schedule: IV

Indications

To prevent or suppress alcohol withdrawal symptoms, act as an adjunct to opioids and analgesics to control postoperative pain , SYRUP, SUPPOSITORIES
Adults.250 mg t.i.d. after meals. Maximum: 2,000 mg. To produce nocturnal sedation , SYRUP, SUPPOSITORIES
Adults.0.5 to 1 g 30 min before bedtime. Maximum: 2 g. To produce preoperative sedation , SYRUP, SUPPOSITORIES
Adults.0.5 to 1 g 30 min before surgery. To provide sedation before dental or medical procedure SYRUP, SUPPOSITORIES Children.25 mg/kg up to 500 mg/single dose; up to 75 mg/kg for dental procedure supplemented by nitrous oxide. Route Onset Peak Duration P.O. 30–60 min Unknown 4–8 hr P.R. Unknown Unknown 4–8 hr

Mechanism of Action

Produces CNS depression by an unknown mechanism involving trichloroethanol, the drug’s active metabolite. chloral hydrate 221

Contraindications

Gastritis; hypersensitivity or idiosyncrasy to chloral hydrate or its components; severe cardiac, hepatic, or renal disease

Interactions

CNS depressants: Increased CNS effects of chloral hydrate furosemide (I.V.): Increased adverse effects when given after chloral hydrate
phenytoin: Increased excretion and decreased effectiveness of phenytoin
warfarin: Transient increase in anticoagulant effect
alcohol use: Increased CNS effects of chloral hydrate

Side Efect

CNS: Ataxia, disorientation, hangover, incoherence, paranoia, somnolence
GI: Gastric irritation, nausea, vomiting
SKIN: Rash, urticaria
Other: Drug dependence

Cautions

Administer with full glass of water or juice to minimize GI distress from chloral hydrate capsules. Dilute syrup in a halfglass of water, ginger ale, or fruit juice.
WARNING Monitor carefully for hypersensitivity reaction in patients with a history of tartrazine sensitivity.

Suspect physical or psychological dependence if withdrawal of chloral hydrate produces confusion, hallucinations, nausea, nervousness, restlessness, stomach pain, tremor, unusual excitement, or vomiting.

PATIENT SAFTY

Instruct patient to take capsules with a full glass of water or juice or to mix syrup in a half-glass of water, ginger ale, or fruit juice.

Advise patient to avoid hazardous activities until CNS effects of chloral hydrate are known.

Caution patient that drug may be habitforming. Advise taking it exactly as prescribed and not to stop taking it abruptly because withdrawal symptoms could occur.

Instruct patient to notify prescriber right away about stomach pains or tarry stools.

Category

Chemical class: Dichloroacetic acid derivative
Therapeutic class: Antibiotic

Pregnancy category: Not rated

Indications

To treat serious infections for which less potentially dangerous are ineffective or contraindicated

IV

Adults.12.5 mg/kg every 6 hr. Maximum: 4 g daily. Children.50 to 75 mg/kg daily in divided doses every 6 hr. Full-term infants age 2 weeks and over. 12.5 mg/kg every 6 hr or 25 mg/kg every 12 hr. Preterm and full-term infants up to age 2 weeks. 6.25 mg/kg every 6 hr. To treat bacteremia or meningitis

IV

Children.50 to 100 mg/kg daily in divided doses every 6 hr.
DOSAGE ADJUSTMENT Dosage limited to 25 mg/kg daily for infants and children with immature metabolic processes.

Mechanism of Action

Produces a bacteriostatic effect on susceptible organisms by inhibiting protein synthesis, thus preventing amino acids from being transferred to growing polypetide chains.

Contraindications

Hypersensitivity to chloramphenicol or its components

Interactions

alfentanil: Prolonged alfentanil effect chloramphenicol 222 barbiturates: Increased blood barbiturate level; decreased chloramphenicol level blood-dyscrasia–causing (such as captopril and cephalosporins), bone marrow depressants (including colchicine and methotrexate): Increased bone marrow depression chlorpropamide, tolbutamide: Increased hypoglycemic effects clindamycin, erythromycin, lincomycin: Decreased antibacterial effects of these cyclophosphamide: Decreased or delayed activation of cyclophosphamide, increased bone marrow depression hepatic enzyme inducers (including rifampin): Decreased chloramphenicol level hydantoins: Increased blood hydantoin level, possibly resulting in toxicity; increased or decreased blood chloramphenicol level iron salts: Increased serum iron level oral anticoagulants: Enhanced anticoagulant action oral contraceptives containing estrogen: Decreased contraceptive effect with prolonged chloramphenicol use penicillins: Decreased penicillin activity; synergistic effects with treatment of certain microorganisms vitamin B12: Antagonized hematopoietic response to vitamin B12

Side Efect

CNS: Confusion, delirium, depression, fever, headache, peripheral neuropathy
CV: Gray syndrome in neonates
EENT: Optic neuritis
GI: Diarrhea, nausea, vomiting
HEME: Aplastic anemia, bone marrow depression, granulocytopenia, hypoplastic anemia, leukopenia, reticulocytopenia, thrombocytopenia
SKIN: Rash
Other: Anaphylaxis, angioedema

Cautions

As appropriate and ordered, obtain specimen for culture and sensitivity testing before starting chloramphenicol therapy.

Keep in mind that chloramphenicol should never be used to treat minor infections or as prophylaxis because of its many serious toxicities.

Repeated courses of therapy should be avoided because of the risk of serious

Side Efect

.

For I.V. use, prepare a 10% solution by adding 10 ml sterile water for injection or D5W to each 1-g vial. Administer over at least 1 minute.

Know that diluted I.V. solution is stable for 24 to 48 hours when stored at room temperature or refrigerated. Don’t use if cloudy.

Assess patient for fever, sore throat, tiredness, unusual bleeding, or ecchymosis; these may indicate a blood dyscrasia.

Perform neurologic assessments regularly, looking for signs of peripheral neuropathy.
WARNING If early signs of gray syndrome appear (failure to eat, pallor, cyanosis, abdominal distention, irregular respirations, and vasomotor collapse), notify prescriber and be prepared to stop drug immediately.

Monitor blood chloramphenicol level as appropriate. Keep in mind that therapeutic peak levels are 10 to 20 mcg/ml and trough levels are 5 to 10 mcg/ml.

Monitor CBC and platelet and reticulocyte counts as ordered to detect signs of blood dyscrasia. Notify prescriber immediately about abnormal results.

PATIENT SAFTY

Instruct patient to immediately report to prescriber signs of blood dyscrasia.
WARNING Tell patient to stay alert for signs of potentially fatal, irreversible bone marrow depression that leads to aplastic anemia and is characterized by fever, pallor, pharyngitis, severe fatigue and weakness, and unusual bleeding or bruising. Bone marrow depression may occur weeks to months after therapy stops. Stress the need for follow-up care.

Category

Chemical class: Benzodiazepine
Therapeutic class: Antianxiety

Pregnancy category: Not rated

Controlled substance schedule: IV chlordiazepoxide hydrochloride 223 C

Indications

To provide short-term management of mild anxiety ,
Adults.5 to 10 mg t.i.d. or q.i.d. Children over age 6. 5 mg b.i.d. to q.i.d. increased as needed to 10 mg b.i.d. or t.i.d., or 0.5 mg/kg daily in equally divided doses every 6 to 8 hr. To provide short-term management of severe anxiety ,
Adults. 20 to 25 mg t.i.d. or q.i.d. I.V.OR
I.M.INJECTION
Adults. Initial: 50 to 100 mg. Then, 25 to 50 mg t.i.d. or q.i.d., p.r.n. Maximum: 300 mg daily.
I.M.INJECTION Children age 12 and over.0.5 mg/kg daily in equally divided doses every 6 to 8 hr. To provide short-term treatment of acute alcohol withdrawal ,, I.V.OR
I.M.INJECTION
Adults. Initial: 50 to 100 mg, usually given I.V. or I.M. Repeated in 2 to 4 hr followed by individualized oral dosage if needed to control symptoms. Maximum: 300 mg daily. To provide perioperative relaxation and reduce apprehension and anxiety ,,
I.M.INJECTION
Adults. 5 to 10 mg P.O. t.i.d. or q.i.d. several days before surgery; 50 to 100 mg I.M. 1 hr before surgery.
DOSAGE ADJUSTMENT Dosage reduced to 5 mg P.O. b.i.d. to q.i.d., p.r.n., for elderly or debilitated patients.

Mechanism of Action

May potentiate the effects of gammaaminobutyric acid (GABA) and other inhibitory neurotransmitters by binding to specific benzodiazepine receptors in limbic and cortical areas of the CNS. By binding to these receptors, chlordiazepoxide increases GABA’s inhibitory effects and blocks cortical and limbic arousal, which helps control emotional behavior. It also helps relieve symptoms of alcohol withdrawal by causing CNS depression.

Contraindications

Hypersensitivity to chlordiazepoxide or its components

Interactions

antacids: Altered rate of chlordiazepoxide absorption cimetidine, disulfiram, fluoxetine, isoniazid, ketoconazole, metoprolol, oral contraceptives, propoxyphene, propranolol,
valproic acid: Increased blood chlordiazepoxide level
CNS depressants: Increased CNS effects digoxin: Increased blood digoxin level and risk of digitalis toxicity levodopa: Decreased efficacy of levodopa’s antiparkinsonian effects neuromuscular blockers: Potentiated, counteracted, or diminished effects of neuromuscular blockers
phenytoin: Possibly increased phenytoin toxicity probenecid: Shortened onset of action or prolonged effect of chlordiazepoxide
rifampin: Decreased chlordiazepoxide effect theophyllines: Antagonized sedative effects of chlordiazepoxide
alcohol use: Increased CNS effects

Side Efect

CNS: Ataxia, confusion, depression, drowsiness, suicidal ideation
CV: ECG changes, hypotension, tachycardia
GI: Hepatic dysfunction
HEME: Agranulocytosis
SKIN: Jaundice
Other: Injection site pain, redness, and swelling

Cautions

Use chlordiazepoxide cautiously in patients with renal or hepatic impairment or porphyria.
WARNING Be aware that prolonged use of chlordiazepoxide at therapeutic doses can lead to dependence.

For I.V. use, reconstitute ampule contents with 5 ml sterile water for injection or sodium chloride for injection. Agitate gently until completely dissolved. Give slowly over 1 minute.

For I.M. use, reconstitute only with diluent provided by manufacturer.
WARNING Don’t use supplied diluent to prepare drug for I.V. use because air bubbles form on the surface.

Don’t give opalescent or hazy solution.

Monitor patient for evidence of phlebitis chlordiazepoxide hydrochloride 224 or thrombophlebitis after I.V. chlordiazepoxide administration.

Monitor liver function test results during therapy.

If patient is a hyperactive, aggressive child or has a history of psychiatric disorders, watch for paradoxical reactions, such as excitement, stimulation, and acute rage, during first 2 weeks of therapy.

Watch patients closely (especially children, adolescents, and young adults) for suicidal tendencies, particularly when chlordiazepoxide therapy starts and dosage changes.

PATIENT SAFTY

Warn that drug may cause drowsiness.

Advise patient to avoid other CNS depressants during therapy.

Warn patient not to take antacids with chlordiazepoxide.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes and particularly if patient is a child, teenager, or young adult.

Category

Chemical class: Sulfonamide derivative
Therapeutic class: Antihypertensive, diuretic

Pregnancy category: B

Indications

To treat hypertension ORAL SUSPENSION,
Adults. 250 to 1,000 mg daily in a single dose or divided doses b.i.d. Maximum: 2,000 mg daily in divided doses. Children age 6 months and over.10 to 20 mg/kg daily in a single dose or divided doses b.i.d. Maximum: 1,000 mg daily for ages 2 to 12; 375 mg daily for ages 6 months to 2 years. Children under age 6 months.Up to 30 mg/kg daily in divided doses given b.i.d. To produce diuresis ORAL SUSPENSION,
Adults. 250 mg every 6 to 12 hr. Administered on an intermittent schedule, if needed, such as alternate days or 3 to 5 days/wk. Children age 6 months and over.10 to 20 mg/kg daily in a single dose or divided doses b.i.d. Maximum: 1,000 mg daily for children ages 2 to 12; 375 mg daily for children ages 6 months to 2 years. Children under age 6 months.Up to 33 mg/kg daily in divided doses b.i.d.
IV: OR INJECTION
Adults.250 mg every 6 to 12 hr. Route Onset Peak Duration P.O. 2 hr 4 hr 6–12 hr I.V. 15 min 4 hr 6–12 hr

Mechanism of Action

May promote sodium, chloride, and water excretion by inhibiting sodium reabsorption in the kidneys’ distal tubules. Initially, chlorothiazide may reduce blood pressure by decreasing extracellular fluid volume, plasma volume, and cardiac output. It also may dilate arteries directly, reducing peripheral vascular resistance. After several weeks, extracellular fluid and plasma volume and cardiac output return to normal, but peripheral vascular resistance remains decreased.

Contraindications

Anuria; hepatic coma; hypersensitivity to chlorothiazide or its components, sulfonamides, or related thiazide diuretics; renal failure

Interactions

allopurinol: Increased risk of allopurinol hypersensitivity amiodarone: Increased risk of arrhythmias from hypokalemia amphotericin B, glucocorticoids: Intensified electrolyte depletion anesthetics: Potentiated effects of anesthetics anticholinergics: Increased chlorothiazide absorption anticoagulants, methenamines, sulfonylureas: Decreased effects of these antihypertensives: Increased antihypertensive effect antineoplastics: Prolonged antineoplasticinduced leukopenia chlorothiazide 225 C calcium: Possibly increased blood calcium level cholestyramine, colestipol: Decreased chlorothiazide absorption diazoxide: Hyperglycemia, hypotension digitalis glycosides: Increased risk of digitalisinduced arrhythmias dopamine: Increased diuretic effect lithium: Increased risk of lithium toxicity loop diuretics: Synergistic effects, resulting in profound diuresis and serious electrolyte imbalances methyldopa: Potential development of hemolytic anemia neuromuscular blockers: Increased neuromuscular blockade
NSAIDs: Possibly reduced diuretic effect of chlorothiazide; increased risk of renal failure if patient has compromised renal function sympathomimetics: Possibly inhibited antihypertensive effect of chlorothiazide
vitamin D: Enhanced vitamin D action

Side Efect

CNS: Dizziness, headache, paresthesia, restlessness, vertigo, weakness
CV: Orthostatic hypotension
ENDO: Hyperglycemia
GI: Abdominal cramps, anorexia, constipation, diarrhea, gastric irritation, nausea, pancreatitis, vomiting
GU: Glycosuria, hematuria (I.V. form), impotence, interstitial nephritis, renal dysfunction or failure
HEME: Agranulocytosis, aplastic anemia, hemolytic anemia, leukopenia, thrombocytopenia
MS: Muscle spasms
SKIN: Jaundice, photosensitivity, purpura, rash, urticaria
Other: Anaphylactic reactions, hypercalcemia, hyperuricemia, hypochloremic alkalosis, hypokalemia, hypomagnesemia, hyponatremia, hypovolemia

Cautions

Don’t give parenteral form of chlorothiazide by I.M. or subcutaneous route.

For I.V. use, reconstitute with at least 18 ml of sterile water for injection. Discard unused solution after 24 hours. Reconstituted solution is compatible with dextrose solution or normal saline solution for infusion.

Watch I.V. site closely. If extravasation occurs, stop infusion and tell prescriber at once.

Weigh patient daily to assess fluid loss and drug effectiveness. If used to treat hypertension, check blood pressure often; antihypertensive effect may not appear for days.

Assess patient for electrolyte imbalances.

Monitor renal function closely, especially in elderly patients, because risk of toxicity increases with renal impairment.

PATIENT SAFTY

Tell patient to take chlorothiazide early in the day to avoid nocturia and to take it with food or milk if GI distress occurs.

Urge patient to eat a high-potassium diet.

Instruct patient to rise slowly to minimize effects of orthostatic hypotension.

Urge patient to weigh himself at least weekly and to notify prescriber if weight rises or falls by 5 lb (2.25 kg) or more in 2 days.

Tell patient to immediately notify prescriber if he develops weakness, cramps, nausea, vomiting, restlessness, excessive thirst, drowsiness, tiredness, increased heart rate, diarrhea, sudden joint pain, or dizziness.

If patient has diabetes mellitus, tell him to check blood glucose level often. Oral antidiabetic dosage may need to be increased.

Tell patient to avoid prolonged exposure to sun, use sunscreen, and wear protective clothing.

Advise patient to consult prescriber or pharmacist before using alcohol and such OTC as those used for appetite control, colds, cough, hay fever, and sinus problems.

Category

Chemical class: Chemically related to mephenesin
Therapeutic class: Skeletal muscle relaxant

Pregnancy category: Not rated

chlorphenesin carbamate 226

Indications

As adjunct to relieve pain in acute musculoskeletal conditions
Adults.800 mg t.i.d. until desired effect occurs. Maintenance: 400 mg q.i.d or less, p.r.n.

Mechanism of Action

May act on the CNS, rather than directly on skeletal muscle, producing a sedative effect that aids in muscle relaxation.

Contraindications

Hypersensitivity to chlorphenesin or its components

Interactions

CNS depressants: Increased adverse CNS effects
alcohol use: Increased adverse CNS effects

Side Efect

CNS: Confusion, dizziness, drowsiness, headache, insomnia, nervousness, paradoxical stimulation
EENT: Diplopia, transient vision loss
GI: Epigastric discomfort, nausea
Other: Anaphylaxis, drug-induced fever

Cautions

WARNING Use chlorphenesin cautiously in patients hypersensitive to aspirin; it contains tartrazine, which may cause hypersensitivity.

Expect drug therapy to last for no more than 8 weeks because safety beyond this point is unknown.

Provide rest and other pain-relief measures.

PATIENT SAFTY

Because of possible reduced alertness, advise patient to avoid potentially hazardous activities until drug’s CNS effects are known.

Instruct patient to notify prescriber if these symptoms occur: confusion, dizziness, drowsiness, insomnia, nervousness, or paradoxical stimulation.

Tell patient to immediately notify prescriber if he develops a fever or any signs or symptoms of an allergic reaction, such as rash, hives, itching, facial swelling, or difficulty breathing.

Category

Chemical class: Propylamine derivative of phenothiazine
Therapeutic class: Antiemetic, antipsychotic, tranquilizer

Pregnancy category: Not rated

Indications

To manage symptoms of psychotic disorders or control manic manifestations of manic-depression in outpatients
Adults.30 to 300 mg 1 to 3 times daily, with dosage adjusted as needed. Maximum: 1 g daily. ORAL CONCENTRATE, SYRUP,
Adults. 10 mg t.i.d. or q.i.d., or 25 mg b.i.d. or t.i.d. After 1 or 2 days, dose increased by 20 to 50 mg semiweekly until patient is calm. After 2 wk of calmness, dosage gradually reduced to maintenance level of 200 to 800 mg daily in equally divided doses. To control acutely disturbed or manic hospitalized patients
I.M.INJECTION
Adults. 25 mg. Repeated 25 to 50 mg in 1 hr, if needed. Increased gradually over several days up to 400 mg every 4 to 6 hr for severe cases until behavior is controlled. Then, regimen switched to oral form and outpatient dosage. To treat severe behavioral problems in children ORAL CONCENTRATE, SYRUP, Children ages 6 months to 12 years. 0.55 mg/kg every 4 to 6 hr, p.r.n. SUPPOSITORIES Children ages 6 months to 12 years. 1 mg/ kg every 6 to 8 hr, p.r.n.
I.M.INJECTION Children ages 6 months to 12 years. 0.55 mg/kg every 6 to 8 hr. Maximum: 75 mg daily for children ages 5 to 12 years chlorpromazine 227 C or weighing 50 to 100 lb (23 to 45 kg), except in unmanageable cases; 40 mg daily for children up to age 5 or weighing up to 50 lb. To treat nausea and vomiting ORAL CONCENTRATE, SYRUP, Adults and adolescents. 10 to 25 mg every 4 to 6 hr, p.r.n. Children ages 6 months to 12 years. 0.55 mg/kg every 4 to 6 hr, p.r.n.
I.M.INJECTION
Adults.25 mg. If no hypotension occurs, 25 to 50 mg every 3 to 4 hr, p.r.n., until vomiting stops; then drug switched to oral form. Children age 6 months and over.0.55 mg/ kg every 6 to 8 hr, p.r.n. Maximum: 75 mg daily for children ages 5 to 12 or weighing 50 to 100 lb; 40 mg daily for children up to age 5 or weighing up to 50 lb. SUPPOSITORIES Adults and adolescents. 50 to 100 mg every 6 to 8 hr, p.r.n. Children ages 6 months to 12 years.1 mg/ kg every 6 to 8 hr, p.r.n. To provide intraoperative control of nausea and vomiting
I.V.INJECTION
Adults. 25 mg diluted to 1 mg/ml with sodium chloride for injection and given at no more than 2 mg every 2 min. Maximum: 25 mg. Children age 6 months and over. 0.275 mg/ kg diluted to at least 1 mg/ml with sodium chloride for injection and given at no more than 1 mg every 2 min. Maximum: 75 mg/ day for children ages 5 to 12 or weighing 50 to 100 lb; 40 mg daily for children up to age 5 years or weighing up to 50 lb.
I.M.INJECTION
Adults.12.5 mg. Repeated in 30 min if needed and no hypotension occurs. Children age 6 months and over.0.275 mg/ kg. Repeated in 30 min if needed and tolerated. To treat intractable hiccups
Adults. 25 to 50 mg t.i.d. or q.i.d. If hiccups last longer than 2 days, route switched to I.M., as prescribed.
IV:
Adults. 25 to 50 mg diluted in 500 to 1,000 ml of normal saline solution and given at 1 mg/min with patient supine.
I.M.INJECTION
Adults.25 to 50 mg given only if oral route is ineffective. If symptoms persist, route switched to I.V., as prescribed. To provide preoperative relaxation ORAL CONCENTRATE, SYRUP, Adults and adolescents. 25 to 50 mg 2 to 3 hr before surgery. Children ages 6 months to 12 years. 0.55 mg/kg 2 to 3 hr before surgery.
I.M.INJECTION
Adults. 12.5 to 25 mg 1 to 2 hr before surgery. Children age 6 months and over. 0.55 mg/ kg 1 to 2 hr before surgery. To treat acute intermittent porphyria ORAL CONCENTRATE, SYRUP, Adults and adolescents.25 to 50 mg t.i.d. or q.i.d.
I.M.INJECTION
Adults. 25 mg t.i.d. or q.i.d. until oral route is possible. To treat tetanus (usually as adjunct with barbiturates)
IV:
Adults.25 to 50 mg diluted to at least 1 mg/ml and given at no more than 1 mg/ min. Children age 6 months and over. 0.55 mg/ kg every 6 to 8 hr, diluted to at least 1 mg/ ml and given at no more than 1 mg/2 min. Maximum: 75 mg daily for children ages 5 to 12 years or weighing 50 to 100 lb; 40 mg daily for children up to age 5 years or weighing up to 50 lb.
I.M.INJECTION
Adults. 25 to 50 mg t.i.d. or q.i.d. Children age 6 months and over.0.55 mg/ kg every 6 to 8 hr. Maximum: 75 mg daily for children ages 5 to 12 or weighing 50 to 100 lb; 40 mg daily for children up to age 5 years or weighing up to 50 lb.
DOSAGE ADJUSTMENT Dosage possibly reduced for patients with hepatic dysfunction. Dosage reduced to one-third to onehalf the normal adult dosage for elderly or debilitated patients.

Mechanism of Action

Depresses brain areas that control activity and aggression, including the cerebral cortex, hypothalamus, and limbic system, by an unknown mechanism. Prevents nausea and vomiting by inhibiting or blocking dopamine receptors in the medullary chlorpromazine 228 chemoreceptor trigger zone and peripherally by blocking the vagus nerve in the GI tract. May relieve anxiety by indirect reduction in arousal and increased filtering of internal stimuli to the reticular activating system in the brain stem.

Incompatibilities

Don’t mix chlorpromazine with thiopental, atropine, or solutions that don’t have a pH of 4 to 5 because a precipitate will form. Don’t mix chlorpromazine injection with other in a syringe.

Contraindications

Comatose states; hypersensitivity to chlorpromazine, phenothiazines, or their components; use of large amounts of CNS depressants

Interactions

amphetamines: Decreased amphetamine effectiveness, decreased antipsychotic effectiveness of chlorpromazine antacids (aluminum hydroxide or magnesium trisilicate gel): Decreased chlorpromazine absorption and effectiveness barbiturates: Decreased plasma level and, possibly, effectiveness of chlorpromazine
CNS depressants: Prolonged and intensified CNS depression metrizamide: Possibly lowered seizure threshold oral anticoagulants: Decreased anticoagulation
phenytoin: Interference with phenytoin metabolism, increased risk of phenytoin toxicity propranolol: Increased plasma levels of both thiazide diuretics: Possibly increased orthostatic hypotension
alcohol use: Prolonged and intensified CNS depression

Side Efect

CNS: Drowsiness, extrapyramidal reactions (such as dystonia, fever, motor restlessness, pseudoparkinsonism, and tardive dyskinesia), neuroleptic malignant syndrome, seizures
CV: ECG changes, such as nonspecific, usually reversible Qand T-wave changes; orthostatic hypotension; tachycardia
EENT: Blurred vision, dry mouth, nasal congestion, ocular changes (fine particle deposits in lens and cornea) with long-term therapy
ENDO: Gynecomastia, hyperglycemia, hypoglycemia, lactation, moderate breast engorgement
GI: Constipation, ileus, nausea
GU: Amenorrhea, ejaculation disorders, impotence, priapism, urine retention
HEME: Agranulocytosis, aplastic anemia, eosinophilia, hemolytic anemia, leukopenia, pancytopenia, thrombocytopenic purpura
SKIN: Exfoliative dermatitis, jaundice, photosensitivity, tissue necrosis, urticaria

Cautions

Don’t open or crush capsules.

Chlorpromazine shouldn’t be used to treat dementia-related psychosis in the elderly because of an increased risk of death.

Use chlorpromazine cautiously in patients (especially children) with chronic respiratory disorders (such as severe asthma or emphysema) or acute respiratory tract infections because drug has CNS depressant effect. Also use cautiously in patients with cardiovascular, hepatic, or renal disease because of increased risk of developing hypotension, heart failure, and arrhythmias.

Because of chlorpromazine’s anticholinergic effects, use it cautiously in patients with glaucoma. Also use it cautiously in those who are exposed to extreme heat or organophosphate insecticides and those receiving atropine or related .

Protect concentrate from light. Refrigeration isn’t required.

Dilute concentrate in at least 60 ml of diluent just before administering it. Use tomato or fruit juice, milk, simple syrup, orange syrup, a carbonated beverage, coffee, tea, water, or semisolid food, such as pudding and soup.

Protect parenteral solution from light. Solution should be clear and colorless to pale yellow. Discard markedly discolored solution.

Don’t inject drug by subcutaneous route because it can cause severe tissue necrosis.

Wear gloves when working with liquid or injectable form because parenteral solution may cause contact dermatitis. chlorpromazine 229 C

For I.V. injection, dilute chlorpromazine with sodium chloride to a concentration of 1 mg/ml.

Give I.M. injection slowly and deep into upper outer quadrant of buttocks, such as in the gluteus maximus. To minimize hypotensive effects, keep patient lying flat and monitor blood pressure for 30 minutes after injection.
WARNING Stay alert for possible suppressed cough reflex, which increases the risk of the patient’s aspirating vomitus.

Monitor patient for increased sensitivity to drug’s CNS effects if patient has a history of hepatic encephalopathy from cirrhosis.
WARNING If neuroleptic malignant syndrome (hyperpyrexia, muscle rigidity, altered mental status, autonomic instability) develops, notify prescriber immediately and expect to stop drug and start intensive treatment. Watch for recurrence if patient resumes antipsychotic therapy.

PATIENT SAFTY

Instruct patient to swallow capsules whole and not to crush, break, or chew them.

Tell patient not to take drug within 2 hours of an antacid. Allow him to take drug with food or a full glass of milk or water.

If patient uses suppository form, tell him to chill the suppository, moisten it with cold water, and insert it well into rectum.

Tell patient to store oral concentrate at room temperature, away from light, to measure it with the dropper provided, and to dilute it in 4 oz of fluid just before use.

Because of possible drowsiness, dizziness, and blurred vision (especially during the first few days of therapy), advise patient to avoid hazardous activities until drug’s CNS effects are known.

Tell patient to avoid alcohol because of possible additive effects and hypotension.

Advise patient, especially if elderly, to rise slowly from a supine or seated position to avoid dizziness, light-headedness, and fainting.

Tell patient to inform doctors and dentists that he’s taking chlorpromazine before he has surgery, medical tests, or dental work.

Explain that drug may reduce the body’s response to heat and cold; tell patient to avoid temperature extremes, as in a sauna, hot tub, or very cold or hot shower. Remind patient to dress warmly in cold weather.

Warn patient not to take OTC for a cold or an allergy because they can increase the risk of heatstroke and other unwanted effects.

Inform patient that drug increases sensitivity to sunlight; tell him to stay out of the sun as much as possible and to protect his skin.

If patient has dry mouth, suggest sugarless chewing gum, hard candy, and fluids.

Urge patient to report sudden sore throat or other signs of infection.

Category

Chemical class: Sulfonylurea
Therapeutic class: Antidiabetic

Pregnancy category: C

Indications

As adjunct to manage non–insulindependent diabetes when diet alone fails to lower blood glucose level
Adults. Initial: 250 mg daily for 5 to 7 days. After therapy begins, dosage may be adjusted up or down in increments of 50 to 125 mg at intervals of 3 to 5 days to obtain optimal control. Maintenance: 100 to 500 mg daily. Maximum: 750 mg daily.
DOSAGE ADJUSTMENT If patient takes more than 40 units of insulin daily, dosage reduced to half usual insulin dose for first few days of chlorpropamide therapy. Insulin dose can be reduced, depending on response. If patient takes oral antidiabetic drug or less than 40 units of insulin daily, it may be stopped abruptly when chlorpropamide starts. Dosage reduced to half usual dose if patient has mild renal failure because metabolites and unchanged drug are excreted in urine. To avoid hypoglycemic reactions, initial dosage reduced to 100 to 125 mg daily for elderly, debilitated, or malnourished patients and patients with impaired hepatic function. chlorpropamide 230

Mechanism of Action

Lowers blood glucose level by stimulating release of insulin from the pancreas in patients who have functioning beta cells. It also may increase insulin sensitivity in target tissues, which may result in a decrease in liver breakdown of glycogen to glucose or the liver’s production of new glucose. Route Onset Peak Duration P.O. 1 hr 3–6 hr 24–72 hr

Contraindications

Diabetic ketoacidosis (with or without coma), hypersensitivity to chlorpropamide or its components, type I diabetes mellitus

Interactions

androgens, anticoagulants, azole antifungals, chloramphenicol, clofibrate, fenfluramine, fluconazole, gemfibrozil, H2-receptor antagonists, magnesium salts, MAO inhibitors, methyldopa, probenecid, salicylates, sulfinpyrazone, sulfonamides, tricyclic antidepressants, urinary acidifiers: Increased hypoglycemic effect barbiturates: Prolonged barbiturate action beta blockers, calcium channel blockers, cholestyramine, corticosteroids, diazoxide, estrogens, hydantoins, isoniazid, nicotinic acid, oral contraceptives, phenothiazines, rifampin, sympathomimetics, thiazide diuretics, thyroid , urinary alkalinizers: Decreased hypoglycemic effect digitalis glycosides: Increased blood digitalis level oral miconazole: Risk of severe hypoglycemia
alcohol use: Disulfiram-like reaction

Side Efect

ENDO: Hypoglycemia
GI: Anorexia, diarrhea, hunger, nausea, vomiting
HEME: Hemolytic anemia
SKIN: Maculopapular eruptions, photosensitivity, pruritus, urticaria
Other: Disulfiram-like reaction

Cautions

Use chlorpropamide cautiously in patients with renal or hepatic dysfunction; in elderly, debilitated, or malnourished patients; and in those with adrenal or pituitary insufficiency because of increased susceptibility to drug’s hypoglycemic action.

Use chlorpropamide cautiously in patients with glucose 6-phosphate dehydrogenase deficiency because sulfonylureas, such as chlorpropamide, can cause hemolytic anemia.

Monitor patient’s blood glucose level often at start of therapy and during dosage adjustments or changes in patient’s life, such as during stress and illness. Hypoglycemia may be difficult to recognize in elderly patients and those who take betaadrenergic blockers.

Assess patient for hypoglycemia—the most common adverse reaction to chlorpropamide—especially in patients whose caloric intake is deficient, who have just engaged in strenuous or prolonged exercise, who have ingested alcohol, or who take more than one glucose-lowering drug.

Treat hypoglycemia promptly by giving 15 g of simple carbohydrate, such as 4 oz of orange juice or soda or 8 oz of milk. Repeat in 15 minutes, if needed. Because of drug’s long half-life, careful monitoring and frequent feedings are required for 3 to 5 days after a hypoglycemic episode. Hospitalization and I.V. glucose may be needed.

Monitor patients receiving long-term chlorpropamide therapy for secondary failure, which causes loss of blood glucose control despite adherence to prescribed drug therapy and diet and exercise guidelines. If secondary failure occurs, therapy should be discontinued and a different antidiabetic drug substituted.

PATIENT SAFTY

Instruct patient to store chlorpropamide in a sealed container, protected from heat and light.

Tell patient to take chlorpropamide with breakfast.

Stress that drug works with diet and exercise to help control blood glucose level and isn’t a substitute for them.

Tell patient to monitor blood glucose level as instructed.

Instruct patient not to skip meals or exercise excessively.

Teach patient how to recognize and treat hypoglycemia. Tell him to report frequent chlorpropamide 231 C or severe hypoglycemia to prescriber.

Caution patient with confirmed or suspected hypoglycemia not to drive or operate machinery until blood glucose levels return to normal.

Tell patient to take a missed dose as soon as he remembers it unless it’s almost time for the next scheduled dose.

Urge patient to wear or carry medical identification showing that he has diabetes and listing his .

Advise the patient to protect his skin from the sun.

Instruct patient to report about fever, sore throat, dark yellow or brown urine, yellow skin and eyes, bleeding, and bruising.

Category

Chemical class: Phthalimidine derivative of benzenesulfonamide (thiazide-like diuretic)
Therapeutic class: Antihypertensive, diuretic

Pregnancy category: B

Indications

To reduce edema caused by heart failure, hepatic cirrhosis, corticosteroid or estrogen therapy, or renal dysfunction
Adults. Initial: 50 to 100 mg (Thalitone, 30 to 60 mg) daily, 100 mg (Thalitone, 60 mg) every other day, or 150 to 200 mg (Thalitone, 90 to 120 mg) daily or every other day. Maintenance: Individualized; may be lower than initial dosage. To treat hypertension
Adults. Initial: 25 mg daily (Thalitone, 15 mg daily). If response is insufficient, dosage increased to 50 mg daily (Thalitone, 30 to 50 mg daily). If additional control is required, dosage increased to 100 mg daily (except Thalitone) or a second antihypertensive added. Maintenance: Individualized; may be lower than initial dosage.

Mechanism of Action

May promote sodium, chloride, and water excretion by inhibiting sodium reabsorption in the distal tubules of the kidneys. Initially, chlorthalidone may decrease extracellular fluid volume, plasma volume, and cardiac output, which helps explain how it reduces blood pressure. It also may dilate arteries directly, which helps reduce peripheral vascular resistance and blood pressure. After several weeks, extracellular fluid and plasma volume and cardiac output return to normal, but peripheral vascular resistance remains decreased. Route Onset Peak Duration P.O. 2–3 hr 2–6 hr 24–72 hr

Contraindications

Anuria; hypersensitivity to chlorthalidone, other sulfonamides, or their components; renal decompensation

Interactions

allopurinol: Increased risk of allopurinol hypersensitivity amphotericin B, glucocorticoids: Intensified electrolyte depletion anesthetics: Potentiated effects of anesthetics anticholinergics: Increased chlorthalidone absorption antidiabetics, methenamines, oral anticoagulants, sulfonylureas: Decreased effects of these antihypertensives: Potentiated action of antihypertensives and chlorthalidone antineoplastics: Prolonged antineoplasticinduced leukopenia cholestyramine, colestipol: Decreased chlorthalidone absorption diazoxide: Increased risk of hyperglycemia and hypotension digitalis glycosides: Increased risk of digitalis-induced arrhythmias lithium: Decreased renal lithium clearance and increased risk of lithium toxicity loop diuretics: Increased synergistic effects, resulting in profound diuresis and serious electrolyte imbalances methyldopa: Potential development of hemolytic anemia neuromuscular blockers: Increased neuromuscular blockade
NSAIDs: Possibly reduced diuretic effect of chlorthalidone
vitamin D: Enhanced vitamin D action chlorthalidone 232

Side Efect

CNS: Dizziness, headache, insomnia, lightheadedness, paresthesia, restlessness, vertigo, weakness
CV: Orthostatic hypotension, vasculitis
EENT: Yellow vision
ENDO: Hyperglycemia
GI: Abdominal cramps or pain, anorexia, bloating, constipation, diarrhea, gastric irritation, nausea, pancreatitis, vomiting
GU: Decreased libido, impotence
HEME: Agranulocytosis, aplastic anemia, hypoplastic anemia, leukopenia, thrombocytopenia
MS: Gout attacks, muscle spasms
SKIN: Cutaneous vasculitis, exfoliative dermatitis, jaundice, necrotizing vasculitis, photosensitivity, purpura, rash, urticaria
Other: Hyperuricemia

Cautions

Use chlorthalidone cautiously in patients with impaired hepatic function or progressive hepatic disease because minor changes in fluid and electrolyte balance may cause hepatic coma.

Assess BUN, serum electrolyte, uric acid, and blood glucose levels before therapy and periodically throughout therapy. Monitor patient for signs of fluid and electrolyte imbalance.
WARNING Monitor renal function periodically to detect cumulative drug effects, which may cause azotemia in patients with impaired renal function.

PATIENT SAFTY

Stress the importance of taking chlorthalidone even when feeling well.

Tell patient to store drug at room temperature in tightly closed container.

Tell patient to take drug in the morning with food or milk.

To minimize effects of orthostatic hypotension, instruct patient to rise slowly from a seated or lying position.

Advise patient to check blood pressure regularly.

Instruct patient to report signs of low potassium level, such as muscle weakness and fatigue.

Advise patient to protect his skin from the sun.

Urge patient to immediately report sudden joint pain to prescriber because drug can cause sudden gout attacks.

Instruct patient to take a missed dose as soon as he remembers it. If he misses one day in an every-other-day schedule, tell him to take the dose on the off day and then resume usual dosing schedule. Warn against taking double or extra doses.

Category

Chemical class: Benzoxazole derivative
Therapeutic class: Skeletal muscle relaxant

Pregnancy category: C

(Parafon Forte DSC, not rated)

Indications

As adjunct to relieve acute musculoskeletal pain and stiffness
Adults.250 to 750 mg t.i.d. or q.i.d., usually 500 mg t.i.d. or q.i.d., increased or decreased according to patient response. Route Onset Peak Duration P.O. In 1 hr Unknown 3–4 hr

Mechanism of Action

Reduces muscle spasm by inhibiting multisynaptic reflex arcs at the level of the spinal cord and subcortical areas of the brain that are active in producing and maintaining skeletal muscle spasm.

Contraindications

Hypersensitivity or known intolerance to chlorzoxazone or any of its components

Interactions

CNS depressants: Additive CNS depression
alcohol use: Additive CNS depression

Side Efect

CNS: Dizziness, drowsiness, headache, light-headedness, malaise, paradoxical stimulation
GI: Abdominal cramps or pain, constipation, diarrhea, GI bleeding, heartburn, hepatotoxicity, nausea, vomiting
GU: Urine discoloration chlorzoxazone 233 C
HEME: Agranulocytosis, anemia
SKIN: Allergic dermatitis, ecchymosis, petechiae
Other: Anaphylaxis, angioedema

Cautions

If needed, crush chlorzoxazone tablets and mix with food or liquid for easier swallowing.

Assess patients, especially those who have a history of allergies, for evidence of hypersensitivity, such as rash, hives, and itching.
WARNING Monitor patient for signs of hepatotoxicity, including fever, rash, jaundice, and darkened urine. Notify prescriber immediately and expect to discontinue drug if any of these signs or symptoms occur. Monitor patient for abnormal liver function test results, such as elevated AST, ALT, alkaline phosphatase, and bilirubin levels, and expect to discontinue drug, as ordered, if any of these occurs.

Ensure adequate rest, and provide other pain-relief measures as needed.

Institute safety measures to prevent falls or injury (such as raising bed rails and assisting with ambulation) until drug’s full CNS effects are known.

PATIENT SAFTY

Advise patient to take a missed dose of chlorzoxazone as soon as possible unless it’s almost time for the next dose.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to avoid alcohol and other CNS depressants during therapy.

Inform patient that, in rare instances, urine may turn orange or reddish purple during therapy.

Advise patient to store drug in a tightly capped container at room temperature.

Category

Chemical class: Quaternary ammonium anion exchange resin
Therapeutic class: Antihyperlipidemic, antipruritic (cholestasis)

Pregnancy category: Not rated

Indications

As adjunct to reduce serum cholesterol level in patients with primary hypercholesterolemia, to relieve pruritus associated with partial biliary obstruction ORAL SUSPENSION
Adults.Initial: 4 g once or twice daily before meals. Maintenance: 8 to 24 g equally divided and given 2 to 6 times a day. Maximum: 24 g daily when used as antihyperlipidemic and 16 g daily when used as antipruritic. Route Onset Peak Duration P.O. In 1–2 wk* Unknown 2–4 wk

Mechanism of Action

Increases bile acid excretion in feces. The resulting decreased bile acid level increases the activity of the enzyme that regulates cholesterol synthesis in the liver. As a result, the liver increases its cholesterol synthesis to produce more bile acids. However, the liver’s synthesis of cholesterol typically can’t match the amount needed to synthesize bile acids, which reduces the cholesterol level. Also, a decreased cholesterol level causes liver cells to increase their uptake of LDLs, which further reduces the cholesterol level. Cholestyramine may relieve pruritus by decreasing the body’s bile acid level. This reduces the amount of excess bile acids that are deposited in the dermis and that typically cause pruritus in patients with cholestasis.

Contraindications

Complete biliary obstruction (when bile isn’t excreted into intestine), hypersensitivity to cholestyramine or its components

Interactions

chenodiol, digitalis glycosides, fat-soluble vitamins, folic acid, gemfibrozil, penicillin G (oral), phenylbutazone, propranolol (oral), tetracyclines (oral), thiazide diuretics (oral), thyroid hormones, ursodiol, vancomycin (oral): Decreased absorption and effects of cholestyramine 234 * For hypercholesterolemia; in 1 to 3 wk for pruritus. For hypercholesterolemia; 1 to 2 wk for pruritus. these oral anticoagulants: Decreased or increased anticoagulant effect

Side Efect

CNS: Headache, dizziness
GI: Bloating, constipation, diarrhea, epigastric pain, eructation, fecal impaction, flatulence, indigestion, nausea, vomiting

Cautions

Store cholestyramine at room temperature.

Don’t give dry powder because it may cause esophageal distress; mix it in a beverage .
WARNING Be aware that long-term use may increase bleeding tendency from hyperprothrombinemia caused by vitamin K deficiency. If this occurs, patient will require treatment with vitamin K1.

Monitor for deficiencies of fat-soluble vitamins, such as A and D. If long-term therapy prevents absorption of these vitamins, expect to provide supplementation.

PATIENT SAFTY

Urge patient to follow a low-cholesterol, low-fat diet and regular exercise program.

Tell patient to take drug before meals.

Instruct patient to mix dry powder as follows: Place amount of powder needed for dose in any beverage and stir vigorously. Then, vigorously stir in another 2 to 4 oz of beverage. After drinking mixture, rinse glass with more liquid, and swallow it to make sure full dose is taken. Patient also may mix drug in thin soups or moist, pulpy fruits, such as applesauce or crushed pineapple.

Tell patient to drink plenty of fluids and increase bulk in his diet to minimize constipation; remind him to notify prescriber if constipation, nausea, or other adverse GI reactions develop.

Explain that serum cholesterol level will need to be measured often for first few months of therapy and periodically thereafter.

Advise patient to take other at least 1 hour before or 4 to 6 hours after cholestyramine to avoid interference with their absorption.

Tell patient to take a missed dose as soon as he remembers but not to take double or extra doses.

Category

Chemical class: Salicylate
Therapeutic class: Analgesic, antiinflammatory, antipyretic

Pregnancy category: C

(first trimester), Not rated (later trimesters)

Indications

To treat mild to moderate pain, reduce fever LIQUID Adults and adolescents. 435 to 870 mg every 4 hr, p.r.n. Maximum: 5,325 mg daily. Children ages 11 to 12. 435 to 652.5 mg every 4 hr, p.r.n. Maximum: Five doses daily. Children ages 9 to 11. 435 to 543.8 mg every 4 hr, p.r.n. Maximum: Five doses daily. Children ages 6 to 9. 435 mg every 4 hr, p.r.n. Maximum: Five doses daily. Children ages 4 to 6. 326.5 mg every 4 hr, p.r.n. Maximum: Five doses daily. Children ages 2 to 4. 217.5 mg every 4 hr, p.r.n. Maximum: Five doses daily. Children up to age 2. Individualized dosage. Maximum: Five doses daily. To treat rheumatoid arthritis LIQUID Adults and adolescents.870 to 1,740 mg up to four times daily. Children age 12 and younger.107 to 133 mg/kg daily in divided doses. Route Onset Peak Duration P.O. Unknown Several wk* Unknown

Mechanism of Action

Blocks cyclooxygenase, an enzyme needed for prostaglandin synthesis. As mediators in the inflammatory process, prostaglandins cause local vasodilation, swelling, and pain. They also influence pain transmission from the periphery to the spinal cord. By blocking cyclooxygenase and inhibiting prostaglandins, this NSAID decreases inflammatory symptoms and relieves pain. It also choline salicylate 235 C * For rheumatoid arthritis. acts on the heat-regulating center in the hypothalamus and causes peripheral vasodilation, sweating, and heat loss.

Contraindications

Hypersensitivity to nonacetylated salicylates

Interactions

antacids: Increased clearance and decreased blood level of salicylate carbonic anhydrase inhibitors, phenytoin,
valproic acid: Decreased blood levels and therapeutic effects of these corticosteroids: Decreased blood salicylate level, increased salicylate dosage requirements insulin, sulfonylureas: Increased hypoglycemic response methotrexate: Increased therapeutic and toxic effects of methotrexate, especially when given in chemotherapeutic doses oral anticoagulants: Increased blood level of unbound anticoagulant and risk of bleeding salicylate-containing products: Increased plasma salicylate level, possibly to toxic level uricosuric : Decreased uricosuric drug efficacy

Side Efect

CNS: Confusion, dizziness, drowsiness, hallucinations, headache, light-headedness
CV: Tachycardia
EENT: Hearing loss, tinnitus
GI: Constipation, diarrhea, epigastric pain, heartburn, indigestion, nausea, vomiting
HEME: Easy bruising, unusual bleeding

Cautions

Use choline salicylate cautiously in patients with renal impairment.

Don’t give salicylates to children and adolescents with chickenpox or influenza symptoms because of the risk of Reye’s syndrome.
WARNING During high-dose or long-term therapy, watch for salicylate intoxication, (headache, dizziness, tinnitus, hearing loss, confusion, drowsiness, diaphoresis, vomiting, diarrhea, hyperventilation, and possibly CNS disturbance, electrolyte imbalance, respiratory acidosis, hyperthermia, and dehydration). Prepare for induced vomiting, gastric lavage, activated charcoal, and peritoneal dialysis or hemodialysis, as ordered.

PATIENT SAFTY

Tell patient to store drug at room temperature, away from heat, light, and moisture.

Instruct patient to take drug with full glass of water or with food.

Tell patient to take a missed dose as soon as he remembers but to avoid doubling the dose.

If patient has arthritis, explain that optimal drug effects may not occur for 2 to 3 weeks.

Teach patient to recognize and immediately report signs of salicylate toxicity.

Because drug is closely related to aspirin, advise against taking aspirin-containing OTC products during therapy.

Category

Chemical class: Non-halogenated glucocorticoid
Therapeutic class: Antiasthmatic, antiinflammatory

Pregnancy category: C

Indications

To prevent asthma attacks as part of maintenance therapy INHALATION AEROSOL Adults and children age 12 and over using bronchodilator therapy. Initial: 80 mcg b.i.d. Maximum: 160 mcg b.i.d. Adults and children age 12 and over switching from another inhaled corticosteroid.Initial: 80 mcg b.i.d., adjusted to lowest effective dose when stabilized. Maximum: 320 mg b.i.d. Adults and children age 12 and older using oral corticosteroid therapy.Initial and maximum: 320 mcg b.i.d., adjusted to lowest effective dose when stabilized. To treat nasal congestion in seasonal or allergic rhinitis INHALATION AEROSOL Adults and children age 6 and over. 200 mcg daily as 2 sprays in each nostril.

Mechanism of Action

Inhibits cells involved in the asthma inflammatory response, such as mast cells, ciclesonide 236 eosinophils, basophils, lymphocytes, macrophages, and neutrophils. Ciclesonide also inhibits production or secretion of chemical mediators, such as histamine, eicosanoids, leukotrienes, and cytokines. Route Onset Peak Duration InhalaUnknown 4 wk or Several tion longer days

Contraindications

Hypersensitivity to ciclesonide or its components, primary treatment of status asthmaticus or other acute asthma episodes that require intensive measures

Interactions

ketoconazole: Increased exposure time of ciclesonide

Side Efect

CNS: Dizziness, fatigue, headache
EENT: Cataracts, conjunctivitis, dry mouth or throat, dysphonia, glaucoma, hoarseness, nasal congestion, nasopharyngitis, oral candidiasis, pharyngolaryngeal pain, sinusitis
ENDO: Adrenal insufficiency, cushingoid symptoms, decreased bone mineral density, hyperglycemia, slower growth in children
GI: Nausea
MS: Arthralgia, back or limb pain, musculoskeletal chest pain
RESP: Bronchospasm, cough, pneumonia, upper respiratory tract infection
SKIN: Facial edema, urticaria
Other: Angioedema, influenza

Cautions

Use cautiously in patients with tuberculosis; fungal, bacterial, viral, or parasitic infection; ocular herpes simplex; or measles or chickenpox because these conditions may worsen with ciclesonide therapy.

Also use cautiously in patients with a history of increased intraocular pressure, glaucoma, or cataracts because ciclesonide may increase intraocular pressure or cause cataract formation and in patients with major risk factors for decreased bone mineral content, such as prolonged immobilization, family history of osteoporosis, or long-term use of that can reduce bone mass, such as anticonvulsants and oral corticoseroids.

Inspect patient’s oral cavity regularly for abnormalities. Have patient rinse mouth following inhalation of ciclesonide to reduce risk of oral candidiasis. If oral candidiasis occurs, expect to continue ciclesonide therapy, unless severe.

If patient takes a systemic corticosteroid, expect to taper dosage by no more than 2.5 mg/day at weekly intervals, starting 1 week after ciclesonide therapy begins.
WARNING If patient is switched from systemic corticosteroid to ciclesonide, assess for adrenal insufficiency (fatigue, hypotension, lassitude, nausea, vomiting, weakness) early in therapy and whenever patient has infection, stress, trauma, surgery, or other steroid-depleting conditions or procedures. Notify prescriber immediately if signs or symptoms develop.

As prescribed, administer a fast-acting inhaled bronchodilator if an acute asthma attack occurs. Ciclesonide is not a bronchodilator and its action takes longer than needed to abort acute asthma symptoms. If bronchospasm occurs immediately after ciclesonide use, expect to stop drug and start another drug regimen.

Monitor growth in children because ciclesonide may suppress growth

PATIENT SAFTY

Urge patient to use ciclesonide regularly, as prescribed, but not for acute bronchospasm. Also tell her never to increase or decrease the dosage without consulting prescriber.

Tell patient to use ciclesonide only with the actuator supplied with the product. Explain that when the dose indicator shows a red zone in the window, about 20 inhalations are left, indicating a need for a refill. When the indicator shows zero, she should discard the inhaler. Advise against relying solely on the dose indicator, especially if inhaler has been dropped, but to keep track of number of inhalations used.

Instruct patient to use inhaler according to package instructions. Stress need to make sure canister is firmly seated in the plastic mouthpiece adapter before each use and to press inhaler slowly but firmly until it can go no further in the adapter for each spray. Inform patient that she doesn’t need to shake inhaler before use. ciclesonide 237 C

On first use, advise her to spray three times into the air (away from her eyes) looking for a fine mist. If inhaler hasn’t been used for more than 10 days, it should be primed again.

Instruct patient to gargle and rinse her mouth after each dose to help prevent dry mouth and throat, relieve throat irritation, and prevent oral yeast infection.

Tell patient to always replace cap after use, to keep mouthpiece clean, and to clean mouthpiece once a week with a clean, dry tissue or cloth.

Explain that the full effect of drug may not occur for 4 weeks or more.

Stress importance of notifying prescriber if symptoms continue or worsen.

Instruct patient to notify prescriber immediately if asthma attacks don’t respond to bronchodilators during ciclesonide use.

If patient is switching from an oral corticosteroid to ciclesonide, urge her to carry medical identification indicating the need for supplemental systemic corticosteroids during stress or severe asthma attack.

Caution patient to avoid contact with people who have infections because drug suppresses the immune system, increasing the risk of infection. Instruct patient to notify prescriber about exposure to chickenpox, measles, or other infections because additional treatment may be needed.

Category

Chemical class: Quinolinone derivative
Therapeutic class: Phosphodiesterase III inhibitor, platelet aggregation inhibitor

Pregnancy category: C

Indications

To reduce symptoms of intermittent claudication
Adults.100 mg b.i.d. taken at least 30 min before or 2 hr after breakfast and dinner.

Mechanism of Action

May inhibit phosphodiesterase, decreasing phosphodiesterase activity and suppressing cyclic adenosine monophosphate (cAMP) degradation. This action increases cAMP in platelets and blood vessels, which inhibits platelet aggregation and causes vasodilation. This in turn relieves symptoms of claudication.

Contraindications

Heart failure, hypersensitivity to cilostazol or its components

Interactions

diltiazem, erythromycin, itraconazole, ketoconazole, omeprazole: Increased plasma cilostazol level grapefruit: Increased risk of adverse reactions high-fat : Faster cilostazol absorption and increased risk of

Side Efect

smoking: Decreased cilostazol effects by about 20%

Side Efect

CNS: Cerebral hemorrhage, dizziness, headache, paresthesia
CV: Angina, chest pain, hypertension, hypotension, palpitations, peripheral edema, prolonged QT interval, subacute thrombosis, tachycardia, torsades de pointes
EENT: Pharyngitis, rhinitis
ENDO: Diabetes mellitus, hot flashes, hyperglycemia
GI: Abdominal pain, abnormal stool, diarrhea, elevated liver function test results, flatulence, GI hemorrhage, hepatic dysfunction, indigestion, jaundice, vomiting
GU: Elevated BUN level, hematuria
HEME: Agranulocytosis, aplastic anemia, bleeding tendency, decreased platelet count, granulocytopenia, leukopenia, thrombocytopenia
MS: Back pain, myalgia
RESP: Cough, interstitial pneumonia, pulmonary hemorrhage
SKIN: Eruptions, pruritus, rash, StevensJohnson syndrome
Other: Infection, increased blood uric acid level

Cautions

Monitor patient’s vital signs and cardiovascular status closely because cilostazol may cause cardiovascular lesions, which could lead to problems, such as endocarcilostazol 238 dial hemorrhage.

Monitor blood glucose level to detect hyperglycemia. Also assess for signs of type 2 diabetes mellitus, such as polyuria, polydipsia, polyphagia, and fatigue.

PATIENT SAFTY

Instruct patient to take cilostazol on an empty stomach because high-fat can increase the risk of

Side Efect

.

Warn patent to avoid grapefruit juice during therapy because it can increase the risk of

Side Efect

.

Urge patient not to smoke because it decreases drug’s effects.

Explain that assessment of drug effectiveness is based on ability to walk increased distances. Stress that drug effects won’t appear until 2 to 4 weeks after therapy starts and that full effects may take up to 12 weeks.

Category

Chemical class: Imidazole derivative
Therapeutic class: Antiulcer agent, gastric acid secretion inhibitor, H2-receptor antagonist

Pregnancy category: B

Indications

To treat and prevent recurrence of duodenal ulcer

ORALL

, Adults and adolescents. Initial: 800 mg at bedtime, 300 mg q.i.d. with meals and at bedtime, or 400 to 600 mg in morning and at bedtime for 4 to 6 wk. Maintenance: 400 mg at bedtime. Children.20 to 40 mg/kg daily in divided doses q.i.d. with meals and at bedtime. I.V. OR

IM

Adults. Initial: 300 mg every 6 to 8 hr. Dosage increased, if needed, by increasing frequency. Maximum: 2,400 mg daily. To treat active, benign gastric ulcer

ORALL

, Adults and adolescents. 800 mg at bedtime, 300 mg q.i.d. with meals and at bedtime, or 600 mg b.i.d. in morning and at bedtime, or 800 mg at bedtime for up to 8 wk. Children.20 to 40 mg/kg daily in divided doses q.i.d. with meals and at bedtime. I.V. OR

IM

Adults and adolescents.Initial: 300 mg every 6 to 8 hr. Dosage increased, if needed, by increasing frequency. Maximum: 2,400 mg daily. To manage gastroesophageal reflux disease

ORALL

, Adults and adolescents.1,600 mg daily in divided doses (800 mg b.i.d or 400 mg q.i.d.) for up to 12 wk. Children.40 to 80 mg/kg daily in divided doses q.i.d. To treat pathological hypersecretory conditions, such as Zollinger-Ellison syndrome

ORALL

, Adults and adolescents. 300 mg q.i.d. with meals and at bedtime. Given more often, if needed. Maximum: 2,400 mg daily. I.V. OR

IM

Adults and adolescents. Initial: 300 mg every 6 to 8 hr. Dosage increased, if needed, by increasing frequency. Maximum: 2,400 mg daily. To treat heartburn and acid indigestion

ORALL

, Adults and adolescents. Initial: 200 mg with water at onset of symptoms. Maximum: 400 mg every 24 hr for no more than 2 wk unless prescribed.
DOSAGE ADJUSTMENT Oral dosage for all indications reduced to 300 mg every 12 hr (and increased to every 8 hr with caution, if needed) for patients with renal impairment. To prevent stress-related upper GI bleeding during hospitalization

IV

Adults.50 mg/hr by continuous infusion for 7 days.

Mechanism of Action

Blocks histamine’s action at H2-receptor sites on stomach’s parietal cells. This action reduces gastric fluid volume and acidity. cimetidine 239 C Cimetidine also decreases the amount of gastric acid secreted in response to food, caffeine, insulin, betazole, or pentagastrin. Route Onset Peak Duration P.O. Unknown 1–2 hr 4–5 hr I.V., I.M. Unknown Unknown 4–5 hr

Incompatibilities

Don’t mix cimetidine with aminophylline or barbiturates in I.V. solution. Don’t mix drug with pentobarbital sodium in the same syringe.

Contraindications

Hypersensitivity to cimetidine or its components

Interactions

antacids, anticholinergics, metoclopramide: Decreased cimetidine absorption benzodiazepines, calcium channel blockers, carbamazepine, chloroquine, labetalol, lidocaine, metoprolol, metronidazole, moricizine, pentoxifylline, phenytoin, propafenone, propranolol, quinidine, quinine, sulfonylureas, tacrine, theophyllines, triamterene, tricyclic antidepressants, valproic acid,
warfarin: Reduced metabolism and increased blood levels and effects of these , possibly toxicity from these carmustine: Increased carmustine myelotoxicity digoxin, fluconazole: Possibly decreased blood levels of these ferrous salts, indomethacin, ketoconazole, tetracyclines: Decreased effects of these flecainide: Increased flecainide effects fluorouracil: Increased blood fluorouracil level after long-term cimetidine use
ketoconazole: Decreased blood ketoconazole level opioid analgesics: Increased toxic effects of opioid analgesics oral anticoagulants: Increased anticoagulant effect procainamide: Increased blood procainamide level succinylcholine: Increased neuromuscular blockade tocainide: Decreased tocainide effects caffeine: Reduced metabolism and increased blood level and effects of caffeine
alcohol use: Possibly increased blood alcohol level

Side Efect

CNS: Confusion, dizziness, hallucinations, headache, peripheral neuropathy, somnolence
ENDO: Mild gynecomastia if used longer than 1 month
GI: Mild and transient diarrhea
GU: Impotence, transiently elevated serum creatinine level
SKIN: Rash
Other: Pain at I.M. injection site

Cautions

WARNING Be aware that rapid administration of cimetidine can increase risk of arrhythmias and hypotension.

For I.V. injection, dilute cimetidine in normal saline solution to a total volume of 20 ml. Inject over 5 minutes or more.

For intermittent I.V. infusion, dilute cimetidine in at least 50 ml of D5W or other compatible I.V. solution. Infuse over 15 to 20 minutes.

For I.M. injection, don’t dilute cimetidine before administering it.

Be alert for confusion in elderly or debilitated patients who receive cimetidine.

PATIENT SAFTY

Tell patient to use a liquid-measuring device to ensure accurate dose of solution.

Advise patient to avoid alcohol while taking cimetidine to prevent interactions.

Instruct patient to avoid taking antacids within 1 hour of taking cimetidine.

Warn patient that cigarette smoking increases gastric acid secretion and can worsen gastric disease.

Caution patient not to take drug for more than 14 days, unless prescribed.

Category

Chemical class: Calcimimetic
Therapeutic class: Calcium reducer cinacalcet hydrochloride 240

Pregnancy category: C

Indications

To treat secondary hyperparathyroidism in patients with chronic renal disease who are on dialysis
Adults. Initial: 30 mg daily P.O., increased every 2 to 4 wk in sequential doses of 60, 90, 120, and 180 mg daily, as needed. To treat hypercalcemia in patients with parathyroid carcinoma
Adults. Initial: 30 mg daily P.O., increased every 2 to 4 wk in sequential doses of 30 mg b.i.d., 60 mg b.i.d., 90 mg b.i.d., and then 90 mg t.i.d. or q.i.d., as needed to normalize serum calcium level. Route Onset Peak Duration P.O. Unknown 2–6 hr Unknown

Mechanism of Action

Increases sensitivity of calcium-sensing receptors on the surface of parathyroid cells to extracellular calcium. This sensitivity directly reduces parathyroid hormone (PTH) level, which in turn decreases serum calcium level.

Contraindications

Hypersensitivity to cinacalcet or its components

Interactions

amitriptyline, carvedilol, desipramine, flecainide, metoprolol, thioridazine, tricyclic antidepressants (most), vinblastine: Possibly increased blood level of these erythromycin, itraconazole,
ketoconazole: Possibly increased blood cinacalcet level

Side Efect

CNS: Asthenia, dizziness
CV: Arrhythmia, hypertension, hypotension, worsening heart failure
ENDO: Hypocalcemia
GI: Anorexia, diarrhea, nausea, vomiting
MS: Myalgia
SKIN: Rash, urticaria
Other: Allergic reaction, angioedema, noncardiac chest pain

Cautions

Use cinacalcet cautiously in patients with a history of seizures because reduced blood calcium level may lower seizure threshold. Also use cautiously in patients with hepatic insufficiency because cinacalcet metabolism may be reduced.

Monitor patient for hypocalcemia exhibited by cramping, myalgia, paresthesia, seizures, and tetany. Also monitor patient’s blood calcium and phosphorus levels within 1 week after starting therapy or adjusting dosage, and every month or two once maintenance dose is established, as ordered. If hypocalcemia develops, notify prescriber immediately because treatment to raise calcium level will be needed. Treatment may include giving supplemental calcium, starting or increasing dosage of calcium-based phosphate binder or vitamin D sterols, or temporarily withholding cinacalcet.

Be aware that if patient starts or stops therapy with a strong CYP3A4 inhibitor, such as erythromycin, itraconazole, or ketoconazole, cinacalcet dosage may need to be adjusted.

Monitor dialysis patient’s intact PTH levels 1 to 4 weeks after therapy starts or dose is adjusted and then every 1 to 3 months thereafter, as ordered. Expect to reduce dosage or discontinue cinacalcet , as ordered, in a patient whose intact PTH level falls below the target range of 150 to 300 pg/ml.

PATIENT SAFTY

Instruct patient to take cinacalcet with food or shortly after a meal.

Caution patient to take tablet whole and not divide it or crush it.

Review signs and symptoms of hypocalcemia with patient and urge him to notify prescriber of changes.

Category

Chemical class: Quinolone derivative
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat UTI caused by Enterobacter species, Escherichia coli, Klebsiella cinoxacin 241 C species, Proteus mirabilis, or Proteus vulgaris
Adults. 1 g daily in divided doses b.i.d. to q.i.d. for 7 to 14 days.
DOSAGE ADJUSTMENT After initial 500-mg dose, dosage reduced to 250 mg t.i.d. if creatinine clearance is 50 to 80 ml/min/1.73 m2, 250 mg b.i.d. if clearance is 20 to 50 ml/ min/1.73 m2, and 250 mg daily if clearance is less than 20 ml/min/1.73 m2. To prevent UTI in women with a history of chronic UTI
Adults. 250 mg at bedtime for up to 5 mo.

Mechanism of Action

Inhibits the enzyme DNA gyrase, which is responsible for the unwinding and supercoiling of bacterial DNA before it replicates. By inhibiting this enzyme, cinoxacin causes bacterial cells to die.

Contraindications

Hypersensitivity to cinoxacin, other quinolones, or their components

Interactions

antacids that contain aluminum or magnesium, didanosine (chewable tablets, buffered tablets, pediatric powder for oral solution), metal cations (such as iron), multivitamins that contain zinc, sucralfate: Possibly interference with cinoxacin absorption probenecid: Increased blood cinoxacin level
theophylline: Possibly increased blood theophylline level caffeine: Decreased metabolism of caffeine, resulting in increased blood caffeine level

Side Efect

CNS: Dizziness, headache
CV: Edema
EENT: Altered taste
GI: Abdominal cramps, anorexia, diarrhea, elevated liver function test results, nausea, vomiting
GU: Perineal burning
HEME: Eosinophilia
SKIN: Angioedema, photosensitivity, pruritus, rash, urticaria

Cautions

Obtain results of urine culture and sensitivity test before administering first dose of cinoxacin.

Review results of liver function tests, as indicated, during treatment.

Administer drug with food, if needed; food decreases peak blood level but doesn’t change total absorption.

PATIENT SAFTY

Tell patient to take cinoxacin with food, if needed, to avoid GI distress.

Instruct patient to drink 2 to 3 L of fluid daily unless contraindicated.

Tell patient not to take antacids that contain aluminum or magnesium; didanosine chewable tablets, buffered tablets, or pediatric powder for oral solution; sucralfate; metal cations such as iron; or multivitamins that contain zinc for at least 2 hours before or after taking cinoxacin because they can interfere drug’s absorption.

Advise patient to limit caffeine intake while taking cinoxacin because drug may cause caffeine to accumulate in the body.

Advise patient to immediately report edema, rash, or severe adverse GI reactions.

Tell patient to immediately report tendon inflammation, pain, or rupture to prescriber because other in the same class as cinoxacin have caused tendon rupture, requiring drug to be discontinued.

Warn patient about the potential for seizures, which have occurred with other in the same class as cinoxacin.

Category

Chemical class: Fluoroquinolone derivative
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To prevent inhalation anthrax after exposure or to treat inhalation anthrax ORAL SUSPENSION, Adults and adolescents.500 mg every 12 hr for 60 days. Children.15 mg/kg every 12 hr for 60 days. Maximum: 500 mg/dose. ciprofloxacin 242
IV: Adults and adolescents.400 mg every 12 hr for 60 days. Children.10 mg/kg every 12 hr for 60 days. Maximum: 400 mg/dose or 800 mg daily. To treat acute sinusitis caused by gramnegative organisms (including Campylobacter jejuni, Citrobacter diversus, Citrobacter freundii, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Morganella morganii, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Pseudomonas aeruginosa, Serratia marcescens, Shigella flexneri, and Shigella sonnei) and gram-positive organisms (including Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, and Streptococcus pneumoniae) ORAL SUSPENSION,
Adults.500 mg every 12 hr for 10 days.
IV:
Adults. For mild to moderate infections, 400 mg every 12 hr. To treat bone and joint infections caused by susceptible organisms listed above ORAL SUSPENSION,
Adults.For mild to moderate infections, 500 mg every 12 hr for 4 to 6 wk. For severe or complicated infections, 750 mg every 12 hr for 4 to 6 wk.
IV:
Adults. For mild to moderate infections, 400 mg every 12 hr for 4 to 6 wk. For severe or complicated infections, 400 mg every 8 hr. To treat skin and soft-tissue infections caused by susceptible organisms listed above ORAL SUSPENSION,
Adults.For mild to moderate infections, 500 mg every 12 hr for 7 to 14 days. For severe or complicated infections, 750 mg every 12 hr for 7 to 14 days.
IV:
Adults. For mild to moderate infections, 400 mg every 12 hr. For severe or complicated infections, 400 mg every 8 hr. To treat chronic bacterial prostatitis caused by susceptible organisms listed above ORAL SUSPENSION,
Adults.500 mg every 12 hr for 28 days.
IV:
Adults.400 mg every 12 hr. To treat infectious diarrhea caused by susceptible organisms listed above ORAL SUSPENSION,
Adults.500 mg every 12 hr for 5 to 7 days. To treat UTI caused by susceptible organisms listed above ORAL SUSPENSION,
Adults. For acute uncomplicated infections, 100 mg every 12 hr for 3 days. For mild to moderate infections, 250 mg every 12 hr for 7 to 14 days. For severe or complicated infections, 500 mg every 12 hr for 7 to 14 days.
IV:
Adults.For mild to moderate infections, 200 mg every 12 hr. For severe or complicated infections, 400 mg every 12 hr. To treat complicated UTI caused by E. coli, K. pneumoniae, Enterococcus faecalis, P. mirabilis, or P. aeruginosa or acute uncomplicated pyelonephritis caused by E. coli
Adults. 1,000 mg daily for 7 to 14 days. To treat acute cystitis caused by E. coli, P. mirabilis, E. faecalis, or Staphylococcus saprophyticus
Adults.500 mg daily for 3 days. To treat lower respiratory tract infections caused by susceptible organisms listed above ORAL SUSPENSION,
Adults.For mild to moderate infections, 500 mg every 12 hr for 7 to 14 days. For severe or complicated infections, 750 mg every 12 hr for 7 to 14 days.
IV:
Adults.For mild to moderate infections, 400 mg every 12 hr. For severe or complicated infections, 400 mg every 8 hr. To treat intra-abdominal infections caused by susceptible organisms listed above
IV:
Adults.400 mg every 8 hr along with parenteral metronidazole. To treat mild to severe nosocomial pneumonia caused by susceptible organisms listed above ciprofloxacin 243 C
IV:
Adults.400 mg every 8 hr. To treat typhoid fever caused by Salmonella typhi or infectious diarrhea caused by C. jejuni, E. coli, S. flexneri, or S. sonnei ORAL SUSPENSION,
Adults.500 mg every 12 hr for 10 days. To treat uncomplicated urethral or cervical gonococcal infections caused by N. gonorrhoeae ORAL SUSPENSION,
Adults. 250 mg as a single dose.
DOSAGE ADJUSTMENT Dosage reduced to 250 to 500 mg every 12 hr if creatinine clearance is 30 to 50 ml/min/1.73 m2; and to 250 to 500 mg P.O. or 200 to 400 mg I.V. every 18 hr if creatinine clearance is 5 to 29 ml/min/1.73 m2. To treat acute cystitis caused by E. coli or K. pneumoniae (PROQUIN XR)
Adults. 500 mg daily for 3 days with evening meal.

Mechanism of Action

Inhibits the enzyme DNA gyrase, which is responsible for the unwinding and supercoiling of bacterial DNA before it replicates. By inhibiting this enzyme, ciprofloxacin causes bacterial cells to die.

Incompatibilities

Don’t administer parenteral ciprofloxacin with aminophylline, amoxicillin, cefepime, clindamycin, dexamethasone, floxacillin, furosemide, heparin, or phenytoin.

Contraindications

Hypersensitivity to ciprofloxacin, quinolones, or their components

Interactions

antacids, didanosine, iron supplements, sucralfate, multivitamins that contain iron or zinc: Decreased ciprofloxacin absorption cyclosporine: Elevated serum creatinine and blood cyclosporine levels glyburide: Severe hypoglycemia methotrexate: Increased blood methotrexate level and increased risk of toxicity NSAIDs (except acetylsalicylic acid): Increased risk of seizures with high doses of ciprofloxacin oral anticoagulants: Enhanced anticoagulant effects
phenytoin: Increased or decreased blood phenytoin level probenecid: Increased blood ciprofloxacin level and, possibly, toxicity
theophylline: Increased blood level, half-life, and risk of adverse effects of theophylline tizanidine: Increased tizanidine effects caffeine: Increased caffeine effects dairy products: Delayed drug absorption

Side Efect

CNS: Agitation, anxiety, cerebral thrombosis, confusion, dizziness, headache, insomnia, light-headedness, migraine, nightmares, paranoia, peripheral neuropathy, restlessness, seizures, syncope, toxic psychosis
CV: Angina, atrial flutter, cardiopulmonary arrest, cardiovascular collapse, hypertension, MI, orthostatic hypotension, palpitations, phlebitis, tachycardia, torsades de pointes, vasculitis, ventricular ectopy
EENT: Oral candidiasis
GI: Abdominal pain, constipation, diarrhea, elevated liver function test results, flatulence, GI bleeding, hepatic failure or necrosis, hepatitis, indigestion, intestinal perforation, jaundice, nausea, pancreatitis, pseudomembranous colitis, vomiting
GU: Crystalluria, hematuria, increased serum creatinine level, interstitial nephritis, nephrotoxicity, renal calculi, renal failure, urine retention, vaginal candidiasis
HEME: Agranulocytosis, bone marrow depression, hemolytic anemia, lymphadenopathy, pancytopenia
MS: Tendinitis, tendon rupture
SKIN: Erythema multiforme, exfoliative dermatitis, photosensitivity, rash, StevensJohnson syndrome, toxic epidermal necrolysis, urticaria
RESP: Bronchospasm, pulmonary embolism, respiratory arrest
Other: Acidosis, anaphylaxis, angioedema, serum sicknesslike reaction

Cautions

Obtain culture and sensitivity test results, as ordered, before giving ciprofloxacin.

Use drug cautiously in patients with CNS disorders and patients who may be more susceptible to drug’s effect on QT interval, such as those taking Class IA or III antiarciprofloxacin 244 rhythmics or those with uncorrected hypokalemia or a history of QT-interval prolongation.

Dilute I.V. ciprofloxacin concentrate to 1 to 2 mg/ml using D5W or sodium chloride for injection. Don’t dilute solutions that come from manufacturer in D5W before I.V. infusion. Infuse slowly over 1 hour.

Store reconstituted solution up to 14 days at room temperature or refrigerated.

Don’t give oral suspension by feeding tube.

Be aware that and immediate-release tablets aren’t interchangeable and that Proquin XR and Cipro XR aren’t interchangeable.

Patient should be well hydrated during therapy to help prevent alkaline urine, which may lead to crystalluria and nephrotoxicity.

Assess patient’s hepatic, renal, and hematologic functions periodically, as ordered, if he’s receiving prolonged therapy.

Monitor patient closely for diarrhea, which may reflect pseudomembranous colitis. If it occurs, notify prescriber and expect to withhold drug and treat diarrhea.

Assess patient for evidence of peripheral neuropathy. Notify prescriber and expect to stop drug if patient complains of burning, numbness, pain, tingling, or weakness in extremities or if physical examination reveals deficits in light touch, pain, temperature, position sense, vibratory sensation, or motor strength.

Monitor patients (especially children, elderly patients, patients receiving corticosteroids, and patients who have renal failure or who have had a kidney, heart, or lung transplant) for evidence of tendon rupture, such as inflammation, pain, and swelling at the site. Be aware that tendon rupture may occur during or after ciprofloxacin therapy. Notify prescriber about suspected tendon rupture, and have patient rest and refrain from exercise until tendon rupture has been ruled out. If present, expect to provide supportive care as ordered.

Assess patient routinely for signs of rash or other hypersensitivity reactions, even after patient has received multiple doses. Stop drug at first sign of rash, jaundice, or other sign of hypersensivitity, and notify prescriber immediately. Be prepared to provide supportive emergency care.

PATIENT SAFTY

Urge patient to complete the prescribed course of therapy, even if he feels better before it’s finished.

Tell patient not to take drug with dairy products or calcium-fortified juices alone.

Advise patient to take ciprofloxacin 2 hours before or 6 hours after antacids, iron supplements, or multivitamins that contain iron or zinc. Tell him to shake oral suspension for 15 seconds, not to chew microcapsules, and not to split, crush, or chew tablets.

Encourage patient to drink plenty of fluids during therapy to help prevent crystalluria.

Urge patient to avoid caffeinated products because caffeine may accumulate in the body during ciprofloxacin therapy and cause excessive stimulation.

Caution patient to avoid excessive exposure to sunlight or artificial ultraviolet light because severe sunburn may result. Tell patient to notify prescriber if sunburn develops; drug will need to be stopped.

Urge patient to avoid hazardous activities until CNS effects of drug are known.

Advise patient to notify prescriber about changes in limb sensation or movement and about inflammation, pain, or swelling over a joint. Urge patient to rest the affected limb at the first sign of discomfort.

Tell patient to stop taking drug and to notify prescriber at first sign of rash or other hypersensitivity reaction.

Urge patient to report watery, bloody stools to prescriber immediately, even up to 2 months after drug therapy has ended.

Category

Chemical class: Racemic, bicyclic phthalate derivative
Therapeutic class: Antidepressant

Pregnancy category: C

citalopram hydrobromide 245 C

Indications

To treat depression

ORALL

,
Adults.Initial: 20 mg daily. Increased by 20 mg at weekly intervals, as prescribed. Usual: 40 mg daily. Maximum: 60 mg daily.
DOSAGE ADJUSTMENT For elderly patients, maximum dosage is 40 mg daily. Route Onset Peak Duration P.O. 1–wk Unknown Unknown

Mechanism of Action

Blocks serotonin reuptake by adrenergic nerves, which normally release this neurotransmitter from their storage sites when activated by a nerve impulse. This blocked reuptake increases serotonin levels at nerve synapses, which may elevate mood and reduce depression.

Contraindications

Hypersensitivity to citalopram or its components, use within 14 days of MAO inhibitor therapy

Interactions

amitriptyline, bromocriptine, buspirone, clomipramine, dextromethorphan, fluoxetine, fluvoxamine, furazolidone, imipramine, levodopa, lithium, meperidine, naratriptan, nefazodone, paroxetine, pentazocine, phenelzine, procarbazine, selegiline, sertraline, sibutramine, sumatriptan, tramadol, tranylcypromine, trazodone, venlafaxine, zolmitriptan: Possibly enhanced serotonergic effects of citalopram, resulting in agitation, chills, confusion, diaphoresis, diarrhea, fever, hyperreflexia, hypomania, incoordination, myoclonus, or tremor aspirin, NSAIDs,
warfarin: Increased risk of bleeding ranging from ecchymoses to lifethreatening hemorrhage carbamazepine: Possibly increased clearance of citalopram
cimetidine: Possibly increased blood citalopram level desipramine, metoprolol: Increased blood levels of these furazolidone, procarbazine, selegiline: Possibly hyperthermia, rigidity, myoclonus, and extreme agitation progressing to delirium and coma itraconazole, ketoconazole, macrolide antibiotics, omeprazole: Possibly decreased clearance of citalopram
MAO inhibitors: Increased risk of lifethreatening serotonin syndrome or neuroleptic malignant syndrome
warfarin: Possibly increased PT

Side Efect

CNS: Agitation, akathisia, anxiety, asthenia, delirium, dizziness, drowsiness, dyskinesia, fatigue, fever, insomnia, myoclonus, neuroleptic malignant syndrome, seizures, serotonin syndrome, suicidal ideation, tremor
CV: Chest pain, prolonged QT interval, thrombosis, ventricular arrhythmias
EENT: Blurred vision, dry mouth, rhinitis, sinusitis
GI: Abdominal pain, anorexia, diarrhea, GI bleeding, hepatic necrosis, indigestion, nausea, pancreatitis, vomiting
GU: Acute renal failure, anorgasmia, decreased libido, dysmenorrhea, ejaculation disorders, impotence, priapism
HEME: Abnormal bleeding, decreased PT, hemolytic anemia, thrombocytopenia
MS: Arthralgia, myalgia, rhabdomyolysis
RESP: Upper respiratory tract infection
SKIN: Diaphoresis, ecchymosis, erythema multiforme
Other: Anaphylaxis, angioedema, hyponatremia, weight gain or loss

Cautions

WARNING When citalopram dosage increases, monitor patient for possible serotonin syndrome, which may include agitation, chills, confusion, diaphoresis, diarrhea, fever, hyperactive reflexes, poor coordination, restlessness, shaking, talking or acting with uncontrolled excitement, tremor, and twitching. In its most severe form, serotonin syndrome can resemble neuroleptic malignant syndrome, which includes a high fever, muscle rigidity, autonomic instability with possible changes in vital signs, and mental status changes.

Be aware that effective antidepressant therapy may convert depression into mania in predisposed people. If patient develops symptoms of mania, notify prescriber immediately and expect to discontinue citalopram.

Monitor patient with hepatic disease for increased

Side Efect

because drug is extensively metabolized in the liver. citalopram hydrobromide 246

Assess elderly patients and those taking diuretics for signs suggesting syndrome of inappropriate secretion of antidiuretic hormone, including hyponatremia and increased serum and urine osmolarity.

If patient (especially a child or adolescent) takes citalopram for depression, monitor him closely for suicidal tendencies, especially when therapy starts or dosage changes, because depression may worsen at these times.

To stop therapy, expect to reduce dosage gradually to avoid serious adverse reactions.

PATIENT SAFTY

Inform patient that citalopram’s full effects may take up to 4 weeks.

Advise patient not to self-medicate for coughs, colds, or allergies without consulting prescriber because these preparations can increase the risk of

Side Efect

.

Caution patient not to stop citalopram abruptly because doing so may lead to serious

Side Efect

.

If patient (especially a child or adolescent) takes citalopram for depression, urge caregivers to monitor him closely for suicidal tendencies, especially when therapy starts or dosage changes.

Caution against taking OTC NSAIDs, aspirin, or other remedies (including herbal products, such as St. John’s wort) while taking citalopram because they may increase the risk of bleeding.

Urge patient to report sudden, severe, or unusual

Side Efect

promptly to prescriber. Although uncommon, lifethreatening adverse effects may occur.

Category

Chemical class: Macrolide derivative
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To treat pharyngitis and tonsillitis caused by Streptococcus pyogenes ORAL SUSPENSION, Adults and adolescents. 250 mg every 12 hr for 10 days. Children.15 mg/kg daily in divided doses every 12 hr for 10 days. To treat acute maxillary sinusitis caused by Haemophilus influenzae, Moraxella catarrhalis, or Streptococcus pneumoniae ORAL SUSPENSION, Adults and adolescents.500 mg every 12 hr for 14 days. Children.15 mg/kg daily in divided doses every 12 hr for 10 days. Adults and adolescents.1,000 mg every 24 hr for 14 days. To treat acute exacerbations of chronic bronchitis caused by H. influenzae, M. catarrhalis, or S. pneumoniae ORAL SUSPENSION, Adults and adolescents. 250 to 500 mg every 12 hr for 7 to 14 days. Children. 15 mg/kg daily in divided doses every 12 hr for 10 days. Adults and adolescents. 1,000 mg every 24 hr for 7 days. To treat uncomplicated skin and softtissue infections caused by Staphylococcus aureus or S. pyogenes ORAL SUSPENSION, Adults and adolescents.250 mg every 12 hr for 7 to 14 days. Children. 15 mg/kg daily in divided doses every 12 hr for 10 days. To treat pneumonia caused by Chlamydia pneumoniae, Mycoplasma pneumoniae, or S. pneumoniae ORAL SUSPENSION, Adults and adolescents. 250 mg every 12 hr for 7 to 14 days. Children.15 mg/kg daily in divided doses every 12 hr for 10 days. To treat pneumonia caused by H. influenzae ORAL SUSPENSION, Adults and adolescents. 250 mg every 12 hr for 7 days. Children.15 mg/kg daily in divided doses every 12 hr for 10 days. To treat acute otitis media caused by H. influenzae, M. catarrhalis, or S. pneumoniae ORAL SUSPENSION, Children. 15 mg/kg daily in divided doses every 12 hr for 10 days. clarithromycin 247 C To treat active duodenal ulcer caused by Helicobacter pylori ORAL SUSPENSION, Adults and adolescents.500 mg every 8 hr for 14 days with omeprazole 40 mg daily in the morning. Then, omeprazole continued at 20 mg daily in the morning days 15 through 28. Or, 500 mg every 12 hr for 14 days with lansoprazole 30 mg and amoxicillin 1 g every 12 hr for 14 days. To prevent or treat Mycobacterium avium complex in patients with HIV infection ORAL SUSPENSION, Adults and adolescents. 500 mg every 12 hr for 7 to 14 days. Children.7.5 mg/kg every 12 hr. Maximum: 500 mg b.i.d.

Mechanism of Action

Inhibits RNA-dependent protein synthesis in many types of aerobic, anaerobic, grampositive, and gram-negative bacteria. By binding with the 50S ribosomal subunit of the bacterial 70S ribosome, clarithromycin causes bacterial cells to die.

Contraindications

Concurrent therapy with astemizole, cisapride, pimozide, or terfenadine; hypersensitivity to clarithromycin, erythromycin, or any macrolide antibiotic

Interactions

astemizole, disopyramide,
quinidine: Possibly prolonged QT interval or torsades de pointes carbamazepine, other metabolized by cytochrome P450 enzyme system: Increased blood levels of these cisapride, disopyramide, pimozide, quinidine, terfenadine: Increased risk of arrhythmias colchicine: Increased risk of colchicine toxicity digoxin: Increased serum digoxin level dihydroergotamine, ergotamine: Risk of acute ergot toxicity lovastatin, simvastatin: Risk of rhabdomyolysis oral anticoagulants: Potentiated anticoagulant effects rifabutin,
rifampin: Decreased blood clarithromycin level by more than 50%
sildenafil: Possibly prolonged blood sildenafil level
theophylline: Increased blood theophylline level triazolam: Possibly increased CNS effects zidovudine: Decreased blood zidovudine level

Side Efect

CNS: Anxiety, confusion, dizziness, fatigue, hallucinations, headache, insomnia, mania, nightmares, seizures, somnolence, tremor, vertigo
CV: Prolonged QT interval, ventricular arrhythmias
EENT: Altered smell, altered taste, glossitis, hearing loss, oral moniliasis, stomatitis, tinnitus, tongue or tooth discoloration
ENDO: Hypoglycemia
GI: Abdominal pain, diarrhea, indigestion, nausea, pancreatitis, pseudomembranous colitis
GU: Anorexia, elevated BUN level, hepatic dysfunction, vomiting
HEME: Leukopenia, neutropenia, increased prothrombin time, thrombocytopenia
SKIN: Pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, new or worsening myasthenia gravis symptoms, superinfection

Cautions

Expect to obtain a specimen for culture and sensitivity tests before giving first dose.

Use clarithromycin cautiously in patients with renal impairment. Be aware that patients with severe renal impairment may need decreased dosage or prolonged dosage interval and that clarithromycin is not recommended in combination with ranitidine bismuth citrate therapy if patient has a creatinine clearance less than 2.5 ml/min/1.73 m2or a history of acute porphyria.

Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold clarithromycin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

PATIENT SAFTY

Stress the importance of taking the full course of clarithromycin exactly as preclarithromycin 248 scribed, even after feeling better.

Caution patient not to crush or chew tablets.

Advise patient to take drug with food if he takes tablets or has GI distress.

If patient takes suspension form, instruct him not to refrigerate it.

Tell patient to report severe nausea, rash, or itching.

Instruct patient not to take OTC or prescription without consulting prescriber of clarithromycin.

Urge patient to immediately report watery, bloody stools to prescriber, even if they occur up to 2 months after therapy has ended.

Category

Chemical class: Synthetic quaternary ammonium derivative
Therapeutic class: Anticholinergic

Pregnancy category: Not rated

Indications

As adjunct to treat peptic ulcer
Adults.2.5 to 5 mg t.i.d. or q.i.d. 30 to 60 min before meals and at bedtime.
DOSAGE ADJUSTMENT Dosage limited to 2.5 mg t.i.d. before meals for elderly or debilitated patients. Route Onset Peak Duration P.O. 1 hr Unknown Up to 3 hr

Mechanism of Action

Inhibits acetylcholine’s muscarinic actions at postganglionic parasympathetic receptor sites, including smooth muscles, secretory glands, and the CNS. These actions relax smooth muscles and diminish GI, GU, and biliary tract secretions.

Contraindications

Angle-closure glaucoma, benign bladder neck obstruction, hypersensitivity to clidinium bromide or its components, ileus, intestinal atony (elderly or debilitated patients), intestinal obstruction, myasthenia gravis, myocardial ischemia, ocular adhesions between lens and iris, prostatic hypertrophy, renal disease, severe ulcerative colitis, tachycardia, toxic megacolon, unstable cardiovascular status in acute hemorrhage

Interactions

amantadine: Increased risk of clidinium adverse effects atenolol: Increased atenolol effects
CNS depressants: Increased clidinium effects phenothiazines: Decreased antipsychotic effectiveness tricyclic antidepressants: Increased clidinium adverse effects
alcohol use: Increased clidinium effects

Side Efect

CNS: Confusion, dizziness, drowsiness, excitement, fever, headache, insomnia, memory loss, nervousness, weakness
CV: Palpitations, tachycardia
EENT: Blurred vision, cycloplegia, dry mouth, increased intraocular pressure, loss of taste, mydriasis, nasal congestion, pharyngitis, photophobia
GI: Bloating, constipation, dysphagia, heartburn, ileus, nausea, vomiting
GU: Impotence, urinary hesitancy, urine retention
SKIN: Decreased sweating, flushing, rash, urticaria

Cautions

Avoid high doses in patients with ulcerative colitis because clindinium may inhibit intestinal motility and cause or worsen toxic megacolon. Also avoid high doses in patients with hiatal hernia or reflux esophagitis because drug may aggravate esophagitis.

Use drug cautiously in patients with heart failure, arrhythmias, hypertension, autonomic neuropathy, hyperthyroidism, allergies, asthma, or debilitating chronic lung disease.
WARNING Monitor elderly patients for excitement, agitation, drowsiness, and confusion, even with small doses, because these patients are more sensitive to clidinium’s effects. If these reactions occur, notify prescriber and expect to decrease dosage.

Take safety precautions to protect patient from injury from falling. clidinium bromide 249 C

PATIENT SAFTY

Instruct patient to take clidinium exactly as prescribed and not to stop taking it suddenly because it can cause withdrawal symptoms, such as vomiting, diaphoresis, and dizziness.

Advise patient to take drug 30 to 60 minutes before meals.

Tell patient not to store capsules in damp places, such as the bathroom.

Teach patient how to prevent or relieve constipation and dry mouth.

Instruct patient to avoid alcohol and other CNS depressants because they increase the drug’s effects.

Instruct patient to report constipation, vision changes, sore throat, difficulty urinating, and palpitations.

Category

Chemical class: Lincosamide
Therapeutic class: Antibacterial and antiprotozoal antibiotic

Pregnancy category: B

Indications

To treat serious respiratory tract infections caused by anaerobes such as occur with anaerobic pneumonitis, empyema, and lung abscess and those caused by pneumococci, staphylococci, and streptococci; serious skin and soft-tissue infections caused by anaerobes, staphylococci, and streptococci; septicemia caused by anaerobes; intra-abdominal infections caused by anaerobes such as occur with intra-abdominal abscess and peritonitis; infections of the female pelvis and genital tract caused by anaerobes such as occur with endometritis, nongonococcal tubo-ovarian abscess, pelvic cellulitis, and postsurgical vaginal cuff infection; bone and joint infections caused by Staphylococcus aureus; as adjunct therapy in chronic bone and joint infections , Adults and adolescents. For serious infections, 150 to 300 mg every 6 hr; for severe infections, 300 to 450 mg every 6 hr. Children.For serious infections, 8 to 16 mg/kg daily in equally divided doses t.i.d. or q.i.d.; for severe infections, 16 to 20 mg/kg/day in equally divided doses t.i.d. or q.i.d.
IV:,
I.M.INJECTION Adults and adolescents age 16 and over. For serious infections, 600 to 1,200 mg daily in equally divided doses b.i.d. to q.i.d.; for severe infections, 1,200 to 2,700 mg daily in equally divided doses b.i.d. to q.i.d.; for life-threatening infections, 4,800 mg daily in equally divided doses b.i.d. to q.i.d. Children ages 1 month to 16 years. 20 to 40 mg/kg daily in equally divided doses t.i.d. or q.i.d., depending on severity of infection. Neonates less than age 1 month. 15 to 20 mg/kg daily in equally divided doses t.i.d. or q.i.d., depending on severity of infection. To treat vaginal infections caused by Gardnerella or Haemophilus VAGINAL CREAM Nonpregnant
Adults.100 mg (1 applicatorful) into vagina daily, preferably at bedtime, for 3 to 7 consecutive days. Pregnant adults in second or third trimester.100 mg (1 applicatorful) into vagina daily, preferably at bedtime, for 7 consecutive days. To treat acne vulgaris FOAM Adults and adolescents.Apply to affected area daily.

Mechanism of Action

Inhibits protein synthesis in susceptible bacteria by binding to the 50S subunits of clindamycin 250 bacterial ribosomes and preventing peptide bond formation, which causes bacterial cells to die.

Incompatibilities

To prevent physical incompatibility, don’t administer with aminophylline, ampicillin, barbiturates, calcium gluconate, magnesium sulfate, or phenytoin.

Contraindications

Hypersensitivity to clindamycin or lincomycin

Interactions

erythromycin: Possibly blocked access of clindamycin to its site of action kaolin-pectin antidiarrheals: Decreased absorption of oral clindamycin neuromuscular blockers: Increased neuromuscular blockade

Side Efect

CNS: Fatigue, headache
CV: Hypotension, thrombophlebitis (after I.V. injection)
EENT: Glossitis, metallic or unpleasant taste (with high I.V. doses), stomatitis
GI: Abdominal pain, diarrhea, esophagitis, nausea, pseudomembranous colitis, vomiting
GU: Cervicitis, vaginitis, and vulvar irritation (with vaginal form)
HEME: Agranulocytosis, eosinophilia, leukopenia, neutropenia, thrombocytopenic purpura
SKIN: Pruritus, rash, urticaria
Other: Anaphylaxis; induration, pain, or sterile abscess after injection; superinfection

Cautions

Expect to obtain a specimen for culture and sensitivity testing before giving first dose.

Use clindamycin cautiously in patients who have a history of asthma, significant allergies, or GI disease; in those with renal or hepatic dysfunction; and in elderly or atopic patients.
WARNING Don’t give 75and 150-mg capsules to tartrazine-sensitive patients.

Store oral solution for up to 2 weeks at room temperature or reconstituted parenteral solution for up to 24 hours at room temperature.

Give I.V. dose by infusion only; don’t give bolus dose. Dilute 300 mg of clindamycin in 50 ml of diluent and give over 10 minutes. Dilute 600 mg of clindamycin in 100 ml of diluent and give over 20 minutes. Dilute 900 mg of clindamycin in 100 ml of diluent and give over 30 minutes.
WARNING Don’t use diluents that contain benzyl alcohol when clindamycin is to be administered to neonates because a fatal toxic syndrome may occur.

Give I.M. injection deep into large muscle mass, such as the gluteus maximus. Rotate injection sites, and avoid giving more than 600 mg by I.M. injection.

Check I.V. site often for phlebitis and irritation.

For topical foam, wash the affected area with mild soap, let it dry fully, and then apply foam to entire affected area.

Monitor results of liver function tests, CBC, and platelet counts during prolonged therapy.

Observe patient for signs and symptoms of superinfection, such as vaginal itching and sore mouth, which may occur 2 to 9 days after therapy begins.

Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold clindamycin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

PATIENT SAFTY

Tell patient to complete the prescribed course of therapy, even if he feels better before it’s finished.

Instruct patient to take oral clindamycin with at least 8 oz of water to prevent esophageal irritation.

Advise patient to take oral drug with food, if needed, to reduce GI distress.

Tell patient not to refrigerate reconstituted oral solution because it may become thick and difficult to pour and to discard unused drug after 14 days.

If patient will use topical foam, tell him to wash affected area with mild soap, let it dry fully, and then apply foam to entire area. Caution against dispensing foam directly onto hands or face because foam will melt when it contacts warm skin. Instead, patient should dispense amount clindamycin 251 C to be used into the cap or onto a cool surface. Tell patient to pick up a small amount with fingertips and gently massage into affected area until foam disappears. If foam feels warm or looks runny, tell patient to run the can under cold water before dispensing.

Warn patient not to rely on latex or rubber condoms and diaphragms for 72 hours after vaginal treatment because mineral oil in vaginal cream may weaken these items.

Explain that having sexual intercourse after using vaginal cream can increase irritation.

Inform patient that I.M. injection may be painful.

Tell patient to immediately report an inflamed mouth or vagina, and rash or lesions.

Urge patient to immediately report watery, bloody stools to prescriber, even up to 2 months after drug therapy has ended.

Category

Chemical class: Aryloxyisobutyric acid derivative
Therapeutic class: Antihyperlipidemic

Pregnancy category: C

Indications

To treat primary hyperlipidemia (type III) that doesn’t respond to diet, and type IV and type V hyperlipidemia that don’t respond to diet in patients at risk for abdominal pain and pancreatitis
Adults. 1.5 to 2 g daily in divided doses b.i.d. to q.i.d. Route Onset Peak Duration P.O. 2–5 days 3 wk 3 wk

Mechanism of Action

Increases the amount of cholesterol that’s secreted into bile and of bile that’s excreted in the feces. Clofibrate also may increase the activity of lipoprotein lipase, which degrades VLDLs.

Contraindications

Hepatic dysfunction, hypersensitivity to clofibrate, lactation, peptic ulcer, pregnancy, primary biliary cirrhosis, renal dysfunction

Interactions

chenodiol, ursodiol: Counteracted effectiveness of these dantrolene: Decreased plasma protein binding of dantrolene furosemide: Increased furosemide and clofibrate effects insulin, sulfonylureas: Increased antidiabetic effect oral anticoagulants: Increased bleeding tendency oral contraceptives: Decreased effectiveness of clofibrate
phenytoin: Displacement of phenytoin from binding site probenecid: Increased clofibrate effects
rifampin: Decreased clofibrate effects

Side Efect

CNS: Dizziness, drowsiness, fatigue, headache, weakness
CV: Angina, edema, phlebitis
EENT: Stomatitis
GI: Abdominal pain, bloating, diarrhea, flatulence, nausea, vomiting
GU: Decreased libido, decreased urine output, impotence, proteinuria
HEME: Eosinophilia
MS: Arthralgia, myalgia
SKIN: Alopecia, dry skin and hair, pruritus, rash, urticaria
Other: Weight gain

Cautions

Obtain baseline CBC, liver and renal function studies, and cholesterol profile, as ordered.

Use clofibrate cautiously in patients with a history of hepatic disease or jaundice and in those with peptic ulcer disease.

PATIENT SAFTY

Tell patient to take clofibrate with milk or food to reduce GI distress.

Tell patient that repeated laboratory tests will be needed to evaluate serum cholesterol and triglyceride levels.

Stress the importance of diet, exercise, and weight loss to control cholesterol.

Tell patient to report ankle or leg swelling, chest pain, decreased urine output, severe clofibrate 252 GI reactions, and unusual weight gain.

If patient takes an anticoagulant, tell him to watch carefully for signs and symptoms of abnormal bleeding.

If patient takes antidiabetic , instruct him to stay alert for signs of hypoglycemia from interactions with these .

Advise women of childbearing age to use contraception during and for several months after clofibrate therapy because of teratogenic effects.

Category

Chemical class: Dibenzazepine derivative
Therapeutic class: Antiobsessional tricyclic antidepressant

Pregnancy category: C

Indications

To treat obsessive-compulsive disorder ,
Adults. Initial: 25 mg daily. Gradually increased to 100 mg daily in divided doses over 2 wk, then to maximum of 250 mg daily in divided doses over next few weeks. At maximum dose, total daily amount may be given at bedtime. Children age 10 and over.Initial: 25 mg daily. Gradually increased to the lesser of 3 mg/kg daily or 100 mg daily in divided doses over 2 wk, then to maximum of 3 mg/kg daily or 200 mg daily, whichever is less. At maximum dose, total daily amount may be given at bedtime. Route Onset Peak Duration P.O. Unknown 2–4 wk Unknown

Mechanism of Action

May inhibit neuronal reuptake of norepinephrine and serotonin, which may be a factor in normalizing neurotransmission in obsessive-compulsive behavior.

Contraindications

Acute recovery period after MI, hypersensitivity to clomipramine or its components, use of an MAO inhibitor within 14 days

Interactions

anticholinergics: Increased anticholinergic effects barbiturates: Decreased level and effects of clomipramine; additive CNS depression bupropion, cimetidine, haloperidol, H2receptor antagonists, selective serotonin reuptake inhibitors,
valproic acid: Increased blood level and therapeutic and adverse effects of clomipramine carbamazepine: Decreased blood clomipramine level; increased carbamazepine level
clonidine: Severely increased blood pressure and risk of hypertensive crisis
CNS depressants: Increased CNS depression dicumarol: Increased anticoagulant effect grepafloxacin, quinolones, sparfloxacin: Increased risk of life-threatening arrhythmias guanethidine: Antagonized antihypertensive effect of guanethidine levodopa: Delayed absorption and decreased bioavailability of levodopa
MAO inhibitors: Increased risk of seizures, coma, or death rifamycins: Decreased clomipramine level sympathomimetics: Possibly potentiated cardiovascular effects thyroid : Increased effects of thyroid and clomipramine
alcohol use: Increased CNS depression

Side Efect

CNS: Anxiety, confusion, depersonalization, depression, dizziness, drowsiness, emotional lability, fatigue, headache, insomnia, panic reaction, paresthesia, somnolence, suicidal ideation (children and teens), syncope, tremor, unusual dreams, yawning
CV: Orthostatic hypotension, palpitations, tachycardia
EENT: Blurred vision, dry mouth, epistaxis, pharyngitis, rhinitis, sinusitis, unpleasant taste
GI: Abdominal pain, anorexia, constipation, diarrhea, flatulence, increased appetite, indigestion, nausea, vomiting
GU: Dysmenorrhea, ejaculation failure, impotence, urinary hesitancy, urine retention
RESP: Bronchospasm
SKIN: Abnormal skin odor, acne, dermatitis, dry skin, photosensitivity, rash, urticaria
Other: Weight gain clomipramine hydrochloride 253 C

Cautions

Be aware that stopping clomipramine abruptly may cause withdrawal symptoms and worsen disorder.
WARNING Don’t give drug within 14 days of an MAO inhibitor to avoid possible seizures, coma, or death.
WARNING Monitor children and teens closely for evidence of suicidal ideation; clomipra-mine increases the risk in these groups.

PATIENT SAFTY

Tell patient not to use alcohol, barbiturates, or other CNS depressants; clomipramine increases their effects.
WARNING Urge parents to watch their child or teen closely for abnormal thinking or behavior or increased aggression or hostility. Stress the need to notify prescriber if they occur.

Inform male patients about risk of sexual dysfunction while taking drug.

Caution patient that drug may cause drowsiness, especially during initial dosage adjustment.

Warn patient not to stop taking drug abruptly.

Instruct patient to take a missed dose as soon as he remembers unless it’s almost time for the next scheduled dose, in which case he should skip the missed dose. Warn against doubling the next dose.

Teach patient how to prevent photosensitivity reactions.

Tell patient to report difficulty urinating, dizziness, dry mouth, sedation, and mental changes.

Caution patient to avoid hazardous activities until CNS effects of drug are known.

Category

Chemical class: Benzodiazepine
Therapeutic class: Anticonvulsant

Pregnancy category: D

Controlled substance schedule: IV

Indications

To treat Lennox-Gastaut syndrome (type of absence seizure disorder) and akinetic and myoclonic seizures Adults and children over age 10. 1.5 mg daily in divided doses t.i.d. Increased by 0.5 to 1 mg every 3 days, if needed, until seizures are controlled. Maximum: 20 mg daily. Children age 10 and under or weighing less than 30 kg (66 lb). 0.01 to 0.03 mg/kg daily in divided doses b.i.d. or t.i.d. Increased by 0.25 to 0.5 mg every third day up to maintenance dosage. Maintenance: 0.1 to 0.2 mg/kg daily, preferably in three equal doses, or if unequal, with largest dose given at bedtime. Maximum: 0.05 mg/kg daily. To treat panic disorder
Adults. Initial: 0.25 mg b.i.d. Increased, if needed, to 1 mg daily after 3 days. If more than 1 mg daily is required, dosage increased in increments of 0.125 to 0.25 mg b.i.d. every 3 days until panic disorder is controlled or

Side Efect

make further increases undesirable. This maintenance dosage may be given as a single dose at bedtime. Maximum: 4 mg daily.

Mechanism of Action

Prevents seizures by potentiating the effects of gamma-aminobutyric acid (GABA), which is an inhibitory neurotransmitter. Suppresses the spread of seizure activity caused by seizure-producing foci in the cortex, thalamus, and limbic structures.

Contraindications

Acute angle-closure glaucoma, hepatic disease, hypersensitivity to benzodiazepines or their components

Interactions

antianxiety , barbiturates, MAO inhibitors, opioids, phenothiazines, tricyclic antidepressants: Increased CNS depression
alcohol use: Increased CNS depression

Side Efect

CNS: Ataxia, confusion, depression, dizziness, drowsiness, emotional lability, fatigue, headache, memory loss, nervousness, reduced intellectual ability, suicidal ideation
CV: Palpitations clonazepam 254
EENT: Blurred vision, eyelid spasm, increased salivation, loss of taste, pharyngitis, rhinitis, sinusitis
GI: Abdominal pain, anorexia, constipation
GU: Difficult ejaculation, dysmenorrhea, dysuria, enuresis, impotence, nocturia, urine retention, UTI
HEME: Anemia, eosinophilia, leukopenia, thrombocytopenia
MS: Dysarthria, myalgia
RESP: Bronchitis, cough
Other: Allergic reaction

Cautions

Use clonazepam cautiously in patients with renal failure, mixed seizure disorder (because drug can increase the risk of generalized tonic-clonic seizures), or respiratory disease and troublesome secretions (because clonazepam increases salivation) and in elderly patients (because they’re more sensitive to drug’s CNS effects).

Monitor blood drug level, CBC, and liver function test results during long-term or high-dose therapy, as ordered.
WARNING Don’t stop drug abruptly; expect to taper dosage gradually to avoid withdrawal symptoms and seizures.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

PATIENT SAFTY

Tell patient to take drug exactly as prescribed. Explain that stopping abruptly can cause seizures and withdrawal symptoms.

Advise patient to avoid alcohol and sleepinducing during therapy. Instruct him to consult prescriber before taking any OTC .

Urge patient to carry medical identification of his seizure disorder and drug therapy.

Warn patient about possible drowsiness.

Instruct patient to report severe dizziness, persistent drowsiness, palpitations, difficulty urinating, seizure activity, and other disruptive

Side Efect

.

Suggest that parents monitor child’s performance in school because clonazepam can cause drowsiness or inattentiveness.

Urge caregivers to watch patient closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes, and to report concerns to prescriber immediately.

Urge female patient who becomes pregnant while taking clonazepam to enroll in the Antiepileptic Drug Pregnancy Registry by calling 1-888-233-2334. Explain that the registry is studying the safety of antiepileptic during pregnancy.

Category

Chemical class: Imidazoline derivative
Therapeutic class: Analgesic, antihypertensive

Pregnancy category: C

Indications

To manage hypertension
Adults. Initial: 0.1 mg b.i.d., increased by 0.1 mg/wk to produce desired response. Maintenance: 0.2 to 0.6 mg daily in divided doses b.i.d. or t.i.d. Maximum: 2.4 mg daily. TRANSDERMAL PATCH
Adults. Initial: 0.1-mg patch applied to hairless area of intact skin on upper arm or torso every 7 days. After 1 to 2 wk, if blood pressure isn’t controlled, two 0.1-mg patches or one 0.2-mg patch applied to skin. Dosage adjusted, as needed, every 7 days. Maximum: Two 0.3-mg patches worn at same time. To treat severe hypertension
Adults.0.2 mg, then 0.1 mg every 1 hr until diastolic blood pressure reaches acceptable range or 0.8 mg has been administered.
DOSAGE ADJUSTMENT Dosage individualized for patients with renal failure. As adjunct to relieve severe pain (in cancer patients) that isn’t adequately relieved by opioid analgesics alone CONTINUOUS EPIDURAL INFUSION
Adults. Initial: 30 mcg/hr. Titrated up or down, if needed, depending on comfort. Maximum: 40 mcg/hr. Children old enough to tolerate placement clonidine 255 C and management of epidural catheter. Initial: 0.5 mcg/kg/hr. Then, titrated to achieve comfort. Route Onset Peak Duration P.O. 30–60 min 2–4 hr 8 hr Trans2–3 days Unknown 7 days dermal

Mechanism of Action

Stimulates peripheral alpha-adrenergic receptors in the CNS to produce transient vasoconstriction and then stimulates central alpha-adrenergic receptors in the brain stem to reduce peripheral vascular resistance, heart rate, and systolic and diastolic blood pressure. May produce analgesia by preventing transmission of pain signals to the brain at presynaptic and postjunctional alpha2-adrenoreceptors in the spinal cord. With epidural administration, clonidine produces analgesia in body areas innervated by the spinal cord segments in which the drug concentrates.

Contraindications

Anticoagulant therapy (epidural infusion); bleeding diathesis; hypersensitivity to clonidine or its components, including adhesive used in transdermal patch; injection site infection (epidural infusion)

Interactions

barbiturates, other
CNS depressants: Increased depressant effects of these beta blockers, calcium channel blockers, digoxin: Additive effects, such as bradycardia and AV block; increased risk of worsened hypertensive response when clonidine is withdrawn (beta blockers only) diuretics, other antihypertensive : Increased hypotensive effect epidural local anesthetics: Prolonged effects of epidural local anesthetics when used with epidural clonidine levodopa: Decreased levodopa effectiveness prazosin, tricyclic antidepressants: Decreased antihypertensive effect of clonidine
alcohol use: Enhanced CNS depressant effects of alcohol

Side Efect

CNS: Agitation, delusional perception, depression, dizziness, drowsiness, fatigue, headache, malaise, nervousness, paresthesia, sedation, syncope, weakness
CV: Arrhythmias, chest pain, congestive heart failure, high-degree AV block, orthostatic hypotension, Raynaud’s phenomenon
EENT: Accommodation disorder, blurred vision, burning eyes, decreased lacrimation, dry eyes and mouth, salivary gland pain
GI: Constipation, hepatitis, mildly elevated liver function test results, nausea, vomiting
GU: Decreased libido, erectile dysfunction, nocturia
HEME: Thrombocytopenia
SKIN: Angioneurotic edema, pruritus, rash, urticaria
Other: Weight gain, withdrawal symptoms

Cautions

Use clonidine cautiously in elderly patients, who may be more sensitive to its hypotensive effect.

Monitor blood pressure and heart rate often during clonidine therapy.

Expect transdermal clonidine to take 2 to 3 days to lower blood pressure.

Remove patch before patient has an MRI to avoid possible burns at the patch site.

Be aware that stopping drug abruptly can elevate serum catecholamine levels and cause such withdrawal symptoms as nervousness, agitation, headache, confusion, tremor, and rebound hypertension.

Expect hypertension to return within 48 hours after drug is discontinued.

PATIENT SAFTY

Advise patient to take drug exactly as prescribed and not to stop abruptly because withdrawal symptoms and severe hypertension may occur.

Instruct patient to consult prescriber if dry mouth or drowsiness becomes a problem during oral clonidine therapy. To minimize these effects, prescriber may suggest taking most of dosage at bedtime.

If a transdermal patch loosens during 7day application period, tell patient to place adhesive overlay directly over patch to ensure adhesion.

Tell patient to rotate transdermal sites.

Instruct patient to remove patch and place a fresh one on another site if skin irritation, redness, or rash develops at patch site. clonidine 256

Advise patient to fold used transdermal patch in half with adhesive sides together and discard it out of the reach of children.

Because of possible sedation, advise patient to avoid hazardous activities until drug’s CNS effects are known.

Advise men that libido may decrease.

Instruct patient to report chest pain, dizziness with position changes, excessive drowsiness, rash, urine retention, and vision changes. As needed, tell patient to rise slowly to avoid hypotensive effects.

Inform patient who wears contact lenses that clonidine may cause dry eyes.

Category

Chemical class: Thienopyridine derivative
Therapeutic class: Platelet aggregation inhibitor

Pregnancy category: B

Indications

To reduce atherosclerotic events, such as stroke and MI, in patients with atherosclerosis documented by recent stroke, MI, or peripheral artery disease
Adults. 75 mg daily. To reduce atherosclerotic events, such as stroke and MI, in patients with acute coronary syndrome (unstable angina or non–Q-wave MI)
Adults.Loading dose: 300 mg. Maintenance: 75 mg daily. To reduce rate of death, reinfarction, or stroke in patients with ST-segment elevation acute MI
Adults.75 mg once daily. Or, loading dose of 300 mg followed by 75 mg once daily.

Mechanism of Action

Binds to adenosine diphosphate (ADP) receptors on the surface of activated platelets. This action blocks ADP, which deactivates nearby glycoprotein IIb/IIIa receptors and prevents fibrinogen from attaching to receptors. Without fibrinogen, platelets can’t aggregate and form thrombi. Route Onset Peak Duration P.O. 2 hr 3–7 days* 5 days

Contraindications

Active pathological bleeding, including peptic ulcer and intracranial hemorrhage; hypersensitivity to clopidogrel or its components

Interactions

aspirin: Increased risk of bleeding CYP2C19 inhibitors, such as cimetidine, esomeprazole, etravirine, felbamate, fluconazole, fluoxetine, fluvoxamine, ketoconazole, omeprazole, ticlopidine, voriconazole: Decreased plasma clopidogrel level, decreased platelet inhibition fluvastatin, phenytoin, tamoxifen, tolbutamide, torsemide: Interference with metabolism of these
NSAIDs: Increased risk of GI bleeding, interference with NSAID metabolism
warfarin: Prolonged bleeding time, interference with warfarin metabolism

Side Efect

CNS: Confusion, depression, dizziness, fatigue, hallucinations, headache
CV: Chest pain, edema, hypercholesterolemia, hypertension, hypotension, vasculitis
EENT: Altered taste; conjunctival, ocular, or retinal bleeding; epistaxis; rhinitis; taste disorders
GI: Abdominal pain; acute liver failure; colitis; diarrhea; duodenal, gastric, or peptic ulcer; elevated liver function test results; gastritis; indigestion; nausea; noninfectious hepatitis; pancreatitis
GU: Elevated serum creatinine level, glomerulopathy, UTI
HEME: Agranulocytosis, aplastic anemia, neutropenia, pancytopenia, prolonged bleeding time, thrombocytopenic purpura, thrombotic thrombocytopenic purpura, unusual bleeding or bruising
MS: Arthralgia, back pain, myalgia
RESP: Bronchitis, bronchospasm, cough, dyspnea, interstitial pneumonitis, upper respiratory tract infection clopidogrel bisulfate 257 C * With repeated doses.
SKIN: Erythema multiforme, lichen planus, pruritus, purpura, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, angioedema, flulike symptoms, serum sickness

Cautions

Avoid clopidogrel in patients who have a genetic variation in CYP2C19 or are receiving CYP2C19 inhibitors. Platelet inhibition may decline, increasing the risk of adverse cardiovascular effects after MI.

Use clopidogrel cautiously in patients with severe hepatic or renal disease, risk of bleeding from trauma or surgery, or conditions that predispose to bleeding (such as peptic ulcer disease or thrombotic thrombocytopenic purpura).

In patient with acute coronary syndrome, expect to give aspirin with clopidogrel.
WARNING Clopidogrel prolongs bleeding time; expect to stop it 5 days before elective surgery.

Obtain blood cell count, as ordered, whenever signs and symptoms suggest a hematologic problem.

Monitor patient who takes aspirin closely because risk of bleeding is increased.

PATIENT SAFTY

Discourage use of NSAIDs, including OTC preparations, during clopidogrel therapy because of potential for bleeding.

Caution patient that bleeding may continue longer than usual. Instruct him to report unusual bleeding or bruising.

Because he has an increased risk of bleeding, urge patient to inform all other health care providers, including dentists, that he takes clopidogrel before having surgery or other procedures or taking a new drug.

Instruct patient to inform his health care providers about his clopidogrel therapy.

Category

Chemical class: Benzodiazepine
Therapeutic class: Alcohol withdrawal adjunct, antianxiety drug, anticonvulsant

Pregnancy category: Not rated

Controlled substance schedule: IV

Indications

To relieve anxiety , Adults and adolescents.Initial: 15 mg at bedtime or 7.5 to 15 mg b.i.d. Dosage adjusted, as needed, to 15 to 60 mg daily in divided doses b.i.d. to q.i.d. Maximum: 90 mg daily. Adults and adolescents.11.25 mg daily as substitute for capsules or tablets in patients who were stabilized on 3.75 mg t.i.d. of those forms; 22.5 mg daily as substitute for capsules or tablets in patients who were stabilized on 7.5 mg t.i.d. of those forms. To relieve symptoms of acute alcohol withdrawal ,
Adults.Initial: 30 mg followed by 15 mg b.i.d. to q.i.d. on day 1 of therapy; 15 mg three to six times on day 2; 7.5 to 15 mg t.i.d. on day 3; 7.5 mg b.i.d. to q.i.d. on day 4; and thereafter, 3.75 mg b.i.d. to q.i.d. Maximum: 90 mg daily. As adjunct to treat partial seizure disorder , Adults and adolescents.Initial: Up to 7.5 mg t.i.d. Increased, if needed, by up to 7.5 mg/wk. Maximum: 90 mg daily. Children ages 9 to 12. Initial: 7.5 mg b.i.d. Increased, if needed, by up to 7.5 mg/wk. Maximum: 60 mg daily. Adults and adolescents.11.25 mg daily as substitute for capsules or tablets in patients who were stabilized on 3.75 mg t.i.d. of those forms; 22.5 mg daily as substitute for capsules or tablets in patients who were stabilized on 7.5 mg t.i.d. of those forms.
DOSAGE ADJUSTMENT Initial dosage reduced to 3.75 to 15 mg daily to treat anxiety in elderly patients.

Mechanism of Action

Potentiates action of gamma-aminobutyric acid (GABA) and other inhibitory neurotransmitters by binding to specific benzodiazepine receptor sites in limbic and cortical areas of CNS, which helps control emotional behavior and suppresses spread of seizure clorazepate dipotassium 258 activity. Drug also helps relieve symptoms of alcohol withdrawal by depressing CNS.

Contraindications

Angle-closure glaucoma, hypersensitivity to chlorazepate or its components

Interactions

barbiturates, MAO inhibitors, opioids, other antidepressants, phenothiazines: Potentiated effects of clorazepate cimetidine, disulfiram, fluoxetine, isoniazid, ketoconazole, metoprolol, oral contraceptives, propoxyphene, propranolol,
valproic acid: Increased blood clorazepate level clozapine: Possibly increased risk of shock
alcohol use: Potentiated clorazepate effects

Side Efect

CNS: Anxiety, ataxia, confusion, depression, dizziness, drowsiness, fatigue, headache, insomnia, irritability, nervousness, psychosis, slurred speech, suicidal ideation, tremor
CV: Hypotension
EENT: Blurred vision, diplopia, dry mouth
GI: Anorexia, constipation, diarrhea, elevated liver function test results, nausea, vomiting
GU: Elevated BUN and serum creatinine levels, incontinence, libido changes, menstrual irregularities, urine retention
HEME: Decreased hematocrit
SKIN: Rash
Other: Drug dependence

Cautions

WARNING Be aware that prolonged use of therapeutic doses can lead to dependence.

Monitor liver function test results during therapy.

Watch closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

PATIENT SAFTY

Tell patient to take clorazepate with food if GI distress occurs.

Advise patient to avoid alcohol and other CNS depressants while taking drug.

Urge patient to avoid hazardous activities until CNS effects of drug are known.

Urge caregivers to watch patient closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes, and to report concerns to prescriber immediately.

Urge female patient who becomes pregnant while taking clorazepate to enroll in the antiepileptic drug pregnancy registry by calling 1-888-233-2334. Explain that the registry is studying the safety of antiepileptic during pregnancy.

Category

Chemical class: Penicillinase-resistant isoxazolyl penicillin derivative
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat mild to moderate upper respiratory tract infections or localized skin and soft-tissue infections caused by penicillinase-producing staphylococci ,,

IV

, I.V. OR

IM

Adults and children weighing 20 kg (44 lb) or more. 250 mg every 6 hr. Maximum: 6 g daily. Children and infants weighing less than 20 kg.50 mg/kg daily in equally divided doses every 6 hr. To treat severe lower respiratory tract infections or disseminated infections caused by penicillinase-producing staphylococci ,,

IV

, I.V. OR

IM

Adults and children weighing 20 kg or more.500 mg every 6 hr. Maximum: 6 g daily. Infants and children weighing less than 20 kg.100 mg/kg daily in divided doses every 6 hr.

Mechanism of Action

Inhibits cell wall synthesis and causes cell lysis and death in bacteria that make rigid, cross-linked cell walls in several steps. Cloxacillin affects the final stage of crosslinking by binding with and inactivating penicillin-binding protein, the enzyme that causes linkage in cell wall strands. cloxacillin sodium 259 C

Incompatibilities

Don’t mix cloxacillin with aminoglycosides because of risk of mutual inactivation.

Contraindications

Hypersensitivity to cloxacillin, penicillin, or their components

Interactions

chloramphenicol, erythromycins, sulfonamides, tetracyclines: Decreased cloxacillin effects hepatotoxic , such as fluconazole: Increased risk of hepatotoxicity methotrexate: Increased blood methotrexate level and risk of toxicity probenecid: Increased and prolonged blood cloxacillin level

Side Efect

CNS: Headache
EENT: Glossitis, oral candidiasis
GI: Abdominal pain, diarrhea, elevated liver function test results, nausea, pseudomembranous colitis, vomiting
GU: Hematuria, vaginal candidiasis
MS: Muscle twitching
SKIN: Pruritus, rash, urticaria
Other: Anaphylaxis

Cautions

Use cloxacillin cautiously in patients hypersensitive to cephalosporins (allergic reaction may be delayed) and those with hypertension (drug is relatively high in sodium).

For I.V. injection, reconstitute 250-mg vial with 4.9 ml of sterile water for injection, 500-mg vial with 4.8 ml, and 2,000-mg vial with 6.8 ml. Shake to dissolve.

For direct I.V. injection, give over 2 to 4 minutes through tubing of a compatible infusing I.V. solution. If giving by intermittent I.V. infusion, further dilute with a suitable diluent (see package insert) and administer over 30 to 40 minutes.

For I.M. injection, reconstitute 250-mg vial with 1.9 ml of sterile water for injection and 500-mg vial with 1.7 ml of sterile water. Shake to dissolve.

Be aware that parenteral solutions are stable 24 hours at room temperature and 72 hours if refrigerated.

PATIENT SAFTY

Tell patient to finish full course of therapy, even if he feels better before drug is gone.

Instruct patient to take oral cloxacillin 1 to 2 hours before meals.

Tell patient to take oral form of cloxacillin with a full glass of water (not fruit juice or soda).

Instruct patient taking oral solution to refrigerate container and to discard unused portion after 14 days. Also instruct him to use a calibrated measuring device to ensure accurate doses.

Advise patient to report signs or symptoms of allergic reaction.

Category

Chemical class: Dibenzodiazepine derivative
Therapeutic class: Antipsychotic

Pregnancy category: B

Indications

To treat severe schizophrenia unresponsive to standard ; to reduce risk of recurrent suicidal behavior in schizophrenia or schizoaffective disorders ORALLY
,
Adults. Initial: 12.5 mg once or twice daily. Increased by 25 to 50 mg daily to 300 to 450 mg daily by the end of 2 wk. Dosage adjustments shouldn’t exceed 100 mg once or twice per wk. Maximum: 900 mg daily. Route Onset Peak Duration P.O. 1–6 hr Unknown 4–12 hr

Mechanism of Action

May produce antipsychotic effects by interfering with dopamine binding to dopamine—especially D4—receptors in the limbic region of the brain and by antagonizing adrenergic, cholinergic, histaminic, and serotoninergic receptors.

Contraindications

Angle-closure glaucoma, coma, history of clozapine-induced agranulocytosis or severe granulocytopenia, hypersensitivity to clozapine or its components, myeloproliferative disorders, severe CNS depression, uncontrolled epilepsy, WBC count below 3,500/mm3 clozapine 260

Interactions

anticholinergics: Potentiated anticholinergic effects benzodiazepines, psychotropics: Additive hypotensive effects; increased risk of cardiopulmonary collapse bone marrow depressants: Potentiated myelosuppressive effects carbamazepine,
phenytoin: Decreased blood clozapine level cimetidine, citalopram, erythromycin: Increased blood clozapine level
CNS depressants: Increased CNS depression digoxin,
warfarin: Increased blood level of digoxin and warfarin; displacement of clozapine from its binding site lithium: Increased risk of confusion, dyskinesia, neuroleptic malignant syndrome, and seizures selective serotonin reuptake inhibitors: Markedly increased blood clozapine level; increased risk of adverse effects and leukocytosis
alcohol use: Increased CNS depression

Side Efect

CNS: Agitation, akinesia, anxiety, ataxia, confusion, depression, dizziness, drowsiness, dystonia, fatigue, fever, headache, hyperkinesia, hypokinesia, insomnia, lethargy, myoclonic jerks, neuroleptic malignant syndrome, nightmares, restlessness, rigidity, sedation, seizures, sleep disturbance, slurred speech, syncope, tardive dyskinesia, tremor, vertigo, weakness
CV: Cardiac arrest, cardiomyopathy, chest pain, deep vein thrombosis, ECG changes, hypercholesterolemia, hypertension, hypertriglyceridemia, hypotension, myocarditis, orthostatic hypotension, tachycardia
EENT: Blurred vision, dry mouth, increased nasal congestion, increased salivation, pharyngitis, tongue numbness or soreness
ENDO: Ketoacidosis, severe hyperglycemia
GI: Abdominal discomfort, anorexia, constipation, diarrhea, elevated liver function test results, heartburn, nausea, vomiting
GU: Abnormal ejaculation; urinary frequency, urgency, and incontinence; urine retention
HEME: Agranulocytosis, eosinophilia, leukopenia, neutropenia
MS: Back or leg pain, muscle spasm or weakness, myalgia
RESP: Dyspnea, respiratory arrest
SKIN: Rash
Other: Weight gain

Cautions

Use clozapine cautiously in patients with hepatic, renal, or cardiovascular disease and in elderly patients with dementiarelated psychosis because they have increased risk of serious or fatal adverse reactions.
WARNING Rarely, clozapine causes severe or life-threatening

Side Efect

, such as agranulocytosis, cardiac or respiratory arrest, deep vein thrombosis, myocarditis (especially in first month), neuroleptic malignant syndrome, and severe hyperglycemia with ketoacidosis in nondiabetic patients. It also may cause seizures and tardive dyskinesia. Monitor patient closely.
WARNING Check patient’s baseline WBC count and absolute neutrophil count (ANC) before therapy and weekly for first 6 months. If WBC count is at least 3,500/mm3and ANC at least 2,000/mm3, check every 2 weeks for next 6 months. If counts remain stable, expect to continue checking every 4 weeks thereafter.

If patient develops mild leukopenia (WBCs 3,000 to 3,500/mm3) or granulocytopenia (ANC 1,500 to 2,000/mm3), expect to check counts twice weekly until normal. In moderate leukopenia (WBCs 2,000 to 3,000/mm3) or granulocytopenia (ANC 1,000 to 1,500/mm3), expect to stop drug temporarily and check counts daily until improved. Follow manufacturer’s direction for resuming drug and monitoring. In severe leukopenia (WBCs less than 2,000/mm3) or granulocytopenia (ANC less than 1,000/mm3), expect to stop drug permanently and monitor counts daily, then as specified by manufacturer.

Monitor temperature. A transient increase above 100.4° F (38° C) may occur, most often within the first 3 weeks of therapy.

When therapy ends, expect to check WBC count and ANC weekly for at least 4 weeks or until WBC count is 3,500/mm3or more and ANC is 2,000/mm3or more.

Monitor patients, especially male patients and younger patients, for dystonia, particularly during the first few days of treatment. Be alert for complaints of neck clozapine 261 C spasms, which sometimes may progress to throat tightness, trouble swallowing or breathing, and tongue protrusion.

PATIENT SAFTY

Tell patient that he’ll receive only a 1-week supply at a time.

Instruct patient taking orally disintegrating tablets (Fazaclo) to leave tablet in blister pack until ready to take it. Tell him to peel foil back to remove tablet (rather than pushing tablet through foil) and then to immediately place tablet in mouth and let it dissolve before swallowing. Explain that no water is needed.

Inform patient that he’ll need weekly blood tests. Review evidence of dyscrasias (fatigue, fever, sore throat, weakness); urge patient to report them to prescriber if they occur.

Instruct patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to rise slowly from lying or sitting position to minimize orthostatic hypotension.

If patient stops drug for more than 2 days, stress need to contact prescriber for instructions; dosage will need to be changed.

Tell patient to consult prescriber before using alcohol or taking OTC .

Advise female patients to notify prescriber if pregnancy occurs or is suspected.

Category

Chemical class: Vitamin K–dependent glycoprotein
Therapeutic class: Antihemophilic, hemostatic

Pregnancy category: C

Indications

To treat bleeding episodes in patients with hemophilia A or B or with inhibitors to Factor VIII or Factor IX
I.V.INJECTION
Adults. 90 mcg/kg as bolus injected over 2 to 5 min every 2 hr until hemostasis achieved; then every 3 to 6 hr, as needed. To prevent bleeding in surgical intervention or invasive procedure in hemophilia A or B patients with inhibitors to factor VIII or factor IX
I.V.INJECTION
Adults.90 mcg/kg as bolus injected over 2 to 5 min immediately before surgery or procedure; then every 2 hr throughout surgery or procedure. After minor surgery: 90 mcg/kg injected over 2 to 5 min every 2 hr for 48 hr; then 90 mcg/kg injected over 2 to 5 min every 2 to 6 hr until healing has occurred. After major surgery: 90 mcg/kg over 2 to 5 min every 2 hr for 5 days; then 90 mcg/kg over 2 to 5 min every 4 hr until healing has occurred. To treat or prevent bleeding episodes in patients with congenital factor VII deficiency
IV:
Adults. 15 to 30 mcg/kg over 2 to 5 min every 4 to 6 hr until hemostasis occurs. To treat patients with acquired hemophilia
IV:
Adults.70 to 90 mcg/kg over 2 to 5 min every 2 to 3 hr until hemostasis occurs.

Mechanism of Action

Activates the extrinsic pathway of coagulation by forming complexes with tissue factor to activate factors IX and X. Activated factor X complexes with other factors to convert prothrombin to thrombin. Thrombin then converts fibrinogen to fibrin, which leads to formation of a hemostatic plug to produce local hemostais. This process may also occur on the surface of activated platelets.

Contraindications

Hypersensitivity to recombinant coagulation factor VIIa, to its components, or to mouse, hamster, or bovine proteins

Interactions

activated and nonactivated prothrombin complex concentrates: Increased risk of thrombosis
warfarin: Possibly reversed warfarin effects

Side Efect

CNS: Fever, headache
CV: Acute MI, bradyarrhythmia, chest tightness or pain, edema, hypertension, coagulation factor VIIa (recombinant) 262 hypotension, supraventricular tachycardia, thrombosis
EENT: Epistaxis
GI: Nausea, vomiting
HEME: Disseminated intravascular coagulation, hemorrhage
MS: Arthralgia
RESP: Wheezing
SKIN: Pruritus, purpura, rash, urticaria
Other: Anaphylaxis, injection site reaction

Cautions

Patients with disseminated intravascular coagulation, advanced atherosclerotic disease, crush injury, septicemia, or concomitant treatment with activated or nonactivated prothrombin complex concentrate are at increased risk for a thrombotic event such as myocardial ischemia or infarction and cerebral ischemia or infarction.

Monitor factor VII–deficient patient’s PT and factor VII coagulant activity before and after giving drug. If factor VIIa activity fails to reach the expected level, the PT isn’t corrected, or bleeding isn’t controlled, notify prescriber. Patient may have developed antibodies to the drug. Be prepared to obtain specimen for antibody analysis.

Reconstitute drug with correct amount of sterile water (2.2 ml for 1.2-mg vial, 4.3 ml for 2.4-mg vial, and 8.5 ml for 4.8-mg vial). Clean the rubber stopper with alcohol, and insert syringe needle into center of the stopper, aiming needle against the side of the vial so a stream of sterile water runs down vial wall. Do not inject diluent directly onto powder. Gently swirl vial until powder is dissolved. Don’t shake reconstituted solution. If solution is foamy, let it settle before giving drug. Once reconstituted, use within 3 hours.

Monitor patient’s clotting status closely. If intravascular coagulation is confirmed by test results or if signs and symptoms occur, notify prescriber and expect to reduce dosage or stop drug.

PATIENT SAFTY

Tell patient to immediately report evidence of allergic reaction, such as hives, rash, chest tightness, or difficulty breathing.

Tell patient that he’ll need regular laboratory tests to check effectiveness of drug.

Category

Therapeutic class: Antitussive, opioid analgesic

Pregnancy category: C

Controlled substance schedule: II

Indications

To treat mild to moderate pain

ORALL

, , I.M. OR SUBCUTANEOUS INJECTION
Adults. 15 to 60 mg (usual, 30 mg) every 4 hr, p.r.n. Children age 1 year or over.0.5 mg/kg every 4 to 6 hr, p.r.n. I.V. INJECTION
Adults.15 to 60 mg (usual, 30 mg) every 4 hr. To treat cough from chemical or mechanical irritation of respiratory system

ORALL

, Adults and adolescents.10 to 20 mg every 4 to 6 hr. Maximum: 120 mg daily. Children ages 6 to 12. 5 to 10 mg every 4 to 6 hr. Maximum: 60 mg daily. Children ages 2 to 6. 2.5 to 5 mg every 4 to 6 hr. Maximum: 30 mg daily. Route Onset Peak Duration P.O. 30–45 min 1–2 hr 4 hr* I.M. 10–30 min 30–60 min 4 hr* SubQ 10–30 min Unknown 4 hr*

Mechanism of Action

May produce analgesia through partial metabolism to morphine. Drug binds with mu, delta, and kappa receptors in the spinal cord and with mu1and kappa3receptors higher in the CNS, decreasing intracellular cAMP, which inhibits adenylate cyclase activity and prevents release of pain neurotransmitters, such as substance P and dopamine, and altering perception of and emotional response to pain. Drug also supcodeine 263 C * For pain; 4 to 6 hr for cough. presses cough by acting on opiate receptors in the cough center.

Contraindications

Hypersensitivity to codeine, other opioids, or their components; significant respiratory depression

Interactions

anticholinergics, paregoric: Increased risk of severe constipation antihypertensives, diuretics: Potentiated hypotensive effects buprenorphine: Decreased codeine effectiveness
CNS depressants: Additive CNS effects hydroxyzine: Increased analgesia; increased CNS depressant and hypotensive effects
MAO inhibitors: Increased risk of unpredictable, severe, and sometimes fatal reactions metoclopramide: Antagonized effect of metoclopramide on GI motility naloxone: Antagonized codeine effect
naltrexone: Precipitated withdrawal symptoms in codeine-dependent patients neuromuscular blockers: Additive respiratory depressant effects other opioids: Additive CNS, respiratory depressant, and hypotensive effects
alcohol use: Additive CNS effects

Side Efect

CNS: Coma, delirium, depression, disorientation, dizziness, drowsiness, euphoria, hallucinations, headache, lack of coordination, lethargy, light-headedness, mental and physical impairment, mood changes, restlessness, sedation, seizures, tremor
CV: Bradycardia, heart block, hypertension, orthostatic hypotension, palpitations, tachycardia
EENT: Altered taste, blurred vision, diplopia, dry mouth, laryngeal edema, laryngospasm, miosis
GI: Abdominal cramps and pain, anorexia, constipation, flatulence, gastroesophageal reflux, ileus, indigestion, nausea, vomiting
GU: Decreased libido, difficult ejaculation, dysuria, impotence, oliguria, ureteral spasm, urinary incontinence, urine retention
MS: Muscle rigidity
RESP: Apnea, bronchoconstriction, bronchospasm, depressed cough reflex, respiratory depression
SKIN: Diaphoresis, flushing, pallor, pruritus, rash, urticaria
Other: Anaphylaxis, facial edema, physical and psychological dependence

Cautions

Evaluate patient for therapeutic response, including decreased pain, cough, and facial grimacing.

Take safety precautions, if needed.

Monitor respiratory depth, effort, and rate. Notify prescriber immediately if respiratory rate drops below 10 breaths/min.

Assess urine output to detect retention.
WARNING Assess patient for evidence of physical and psychological dependence.

Rotate sites for subcutaneous delivery. Repeated injection in same site may cause tissue irritation, pain, and induration.

PATIENT SAFTY

Advise patient to avoid alcohol or other CNS depressants while taking codeine.

To minimize nausea, suggest that patient take drug with food.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Caution patient to get up slowly from a sitting or lying position.

To prevent constipation, urge patient to consume plenty of fluids and high-fiber , if not contraindicated.

Instruct patient to take codeine exactly as prescribed and not to adjust dose or frequency without consulting prescriber.

Advise patient to report shortness of breath or difficulty breathing.

Urge breast-feeding women to notify prescriber before taking codeine because drug appears in breast milk and could lead to overdose in infant.

Category

Chemical class: Colchicum alkaloid derivative
Therapeutic class: Antigout, anti-inflammatory

Pregnancy category: C

(oral form), D (parenteral forms) colchicine 264

Indications

To prevent gouty arthritis attacks (COLCRYS) Adults and adolescents age 16 and over. 0.5 to 0.6 mg once or twice daily. Maximum: 1.2 mg daily.

IV

OR INJECTION
Adults.0.5 to 1 mg once or twice daily. Maximum: 4 mg daily. To treat acute gouty arthritis (COLCRYS)
Adults. Initial: 1.2 mg at first sign of flare; then 0.6 mg 1 hr later. Maximum: 1.8 mg over a 1-hr period.
IV: OR INJECTION
Adults. 2 mg over 2 to 5 min; then 0.5 mg every 6 hr or 1 mg every 6 to 12 hr until pain decreases. Maximum: 4 mg daily.
DOSAGE ADJUSTMENT For elderly patients, maximum I.V. dosage reduced to 2 mg/ 24 hr; maximum oral dosage to 2 mg/24 hr. After initial I.V. course, elderly patient should receive no form of colchicine for 21 days. If treatment of a gout flare occurs during prophylactic treatment, dosage shouldn’t exceed 1.2 mg at the first sign of flare, followed by 0.6 mg 1 hour later, and then prophylactic dose resumed 12 hr later. For patient taking strong CYP3A4 inhibitor (atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin), moderate CYP3A4 inhibitor (amprenavir, aprepitant, diltiazem, ertthromycin, fluconazole, fosamprenavir, grapefruit juice, verapamil), or P-gp inhibitor (cyclosporine, ranolazine), dosage usually halved and not repeated for 3 days. For patient with moderate to severe renal impairment, dosage adjusted on individual basis. For patient with severe hepatic impairment receiving colchicine prophylacticly, dosage decreased on individual basis. For patient with severe hepatic impairment receiving colchicine treatment for acute gout flare but not prophylaxis, dosage not adjusted but treatment course shouldn’t be repeated more than once very 2 weeks. To treat familial Mediterranean fever (FMF) (COLCRYS) Adults and adolescents ages 12 and over. 1.2 mg to 2.4 mg daily, with daily total divided into two doses, if desired. Children ages 6 to 12. 0.9 mg to 1.8 mg daily, with daily total divided into two doses, if desired. Children ages 4 to 6. 0.3 mg to 1.8 mg daily, with daily total divided into two doses, if desired.
DOSAGE ADJUSTMENT For adults needing control of FMF, dosage increased in increments of 0.3 mg daily to a maximum of 2.4 mg daily. For adults with intolerable adverse effects, dosage decreased in increments of 0.3 mg daily to tolerable level. For patients taking strong CYP3A4 inhibitor (atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin), moderate CYP3A4 inhibitor (amprenavir, aprepitant, diltiazem, erythromycin, fluconazole, fosamprenavir, grapefruit juice, verapamil), or P-gp inhibitor (cyclosporine, ranolazine), dosage usually colchicine 265 C Leukocyte exterior Leukocyte interior Cell membrane Microtubule Colchicine Tubulin

Mechanism of Action

In gouty arthritis, leukocytes phagocytose urate crystals in affected joints, a process that releases chemotactic factors, degradation enzymes, and other inflammatory substances. Colchicine helps stop this process, probably by disrupting microtubules in leukocytes. Normally, microtubules contribute to cell structure and movement. When colchicine binds to tubulin (protein from which microtubules are made), the microtubule falls apart, as shown. This process disrupts cell function and prevents leukocytes from invading joints and causing inflammation. halved and not repeated for 3 days. For patient with moderate to severe renal impairment or severe hepatic impairment, dosage adjusted on individual basis. Route Onset Peak Duration P.O. In 12 hr In 24–48 hr Unknown I.V. In 6–12 hr Unknown Unknown

Contraindications

Blood dyscrasias; hypersensitivity to colchicine or its components; serious cardiac, GI, hepatic, or renal disorders

Incompatibilities

Don’t combine colchicine with bacteriostatic agents, any solution or injection that contains D5W, and any other solution that may change colchicine’s pH because precipitation may occur.

Interactions

anticoagulants, such as heparin; platelet aggregation inhibitors, such as aspirin; thrombolytics, such as alteplase: Increased risk of GI ulcers or hemorrhage antineoplastics: Possibly increased serum uric acid level and decreased therapeutic effectiveness of colchicine cyclosporine: Increased cyclosporine level moderate CYP3A4 inhibitors, such as amprenavir, aprepitant, diltiazem, erythromycin, fluconazole, fosamprenavir, grapefruit juice, verapamil: Increased risk of colchicine toxicity NSAIDs, such as phenylbutazone: Possibly increased risk of bone marrow depression, GI bleeding, leukopenia, thrombocytopenia strong CYP3A4 inhibitors, such as atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin: Increased risk of colchicine toxicity P-gp inhibitors, such as cyclosporine, ranolazine: Increased risk of colchicine toxicity vitamin B12: Possibly impaired absorption of and increased dosage requirements for vitamin B12
alcohol use: Increased risk of adverse GI effects

Side Efect

CNS: Peripheral neuropathy
CV: Arrhythmias (I.V. form)
GI: Abdominal pain, anorexia, diarrhea, nausea, vomiting
HEME: Agranulocytosis, aplastic anemia, thrombocytopenia
MS: Myopathy
SKIN: Alopecia, rash
Other: Injection site pain and tenderness, median nerve neuritis in affected arm, and skin and soft-tissue necrosis if extravasation occurs (I.V. form)

Cautions

Patients receiving prophylactic treatment for gout and who have hepatic impairment or are being treated with CYP3A4 inhibitors shouldn’t receive colchicine for acute gout flares.
WARNING Avoid subcutaneous or I.M. administration of colchicine because these routes may cause tissue necrosis and sloughing. To prevent extravasation, make sure I.V. catheter is patent and correctly positioned before giving drug. Throughout therapy, check I.V. injection site often for pain, tenderness, and skin peeling. Consult prescriber about switching to oral form.
WARNING To reduce risk of toxicity, avoid giving colchicine by any route within 7 days after full I.V. course (4 mg). If patient takes any drug that increases risk of colchicine toxicity, expect to wait 3 days after oral therapy before starting second oral course. Elderly or debilitated patients and those with a history of cardiac disease or impaired renal or hepatic function are at increased risk for cumulative toxicity.

Dilute I.V. form with 10 to 20 ml of normal saline solution. Or, give colchicine into a large vein through an I.V. line with normal saline solution infusion.

Administer I.V. form over 2 to 5 minutes.

Expect to monitor CBC and platelet and reticulocyte counts at baseline and every 3 months after therapy starts.

Notify prescriber immediately and expect to stop colchicine if patient develops evidence of toxicity, such as abdominal pain, diarrhea, nausea, or vomiting.

PATIENT SAFTY

Instruct patient to have blood tests every 3 months, as ordered, during therapy.

Explain that gouty arthritis pain and colchicine 266 swelling typically subside in 24 to 48 hours after therapy begins.

Advise patient to notify prescriber immediately if abdominal pain, diarrhea, nausea, or vomiting occurs.

Category

Chemical class: Nonabsorbed hydrogel polymer
Therapeutic class: Bile acid sequestrant

Pregnancy category: B

Indications

As adjunct to diet and exercise to reduce elevated LDL cholesterol levels in patients with primary hypercholesterolemia; as adjunct to diet and exercise to improve glycemic control in type 2 diabetes mellitus
Adults. 3.75 g once daily or 1.875 g b.i.d. with a meal and a beverage.

Mechanism of Action

Binds with bile acids in intestine, preventing their absorption and forming an insoluble complex that’s excreted in feces. This action decreases amount of bile acids returning through enterohepatic circulation to the liver. As a result, the liver must convert more cholesterol to bile acids, which increases liver’s demand for cholesterol. This, in turn, causes increase in production and activity of the hepatic enzyme hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase, which is needed for cholesterol production. However, synthesis of cholesterol in the liver typically can’t match the amount needed to synthesize bile acids. Because cholesterol levels can’t be sustained, LDLs, lipoproteins composed mostly of cholesterol, are increasingly removed from the blood, thereby decreasing the LDL level in the blood.

Contraindications

History of bowel obstruction or pancreatitis induced by hypertriglyceridemia, hypersensitivity to colesevelam or its components, serum triglyceride level greater than 500 mg/dl

Interactions

with narrow therapeutic index, glyburide, levothyroxine, oral contraceptives,
phenytoin: Possibly altered effectiveness of these
warfarin: Reduced INR

Side Efect

CNS: Asthenia
CV: Hypertension, hypertriglyceridemia
EENT: Oral blistering, pharyngitis, rhinitis
ENDO: Hypoglycemia, hypertriglyceridemia
GI: Abdominal distention or pain, bowel or esophageal obstruction, constipation, dyspepsia, elevated liver enzymes, fecal impaction, indigestion, nausea, pancreatitis, worsening of hemorrhoids
MS: Myalgia
SKIN: Rash
Other: Flu syndrome

Cautions

Colesevelam shouldn’t be given to patients with gastroparesis or other GI motility disorders or to patients who had major GI tract surgery and are at risk for bowel obstruction from constipating effects.

Use cautiously in patients with dysphagia or esophageal obstruction because size of tablet can cause dysphagia or esophageal obstruction.

Use colesevelam cautiously in patients whose total triglycerides exceed 300 mg/dl; bile acid sequestrants can increase it.

Evaluate patient’s lipid levels before starting therapy for primary hyperlipidemia, again in 4 to 6 weeks, and then periodically, as ordered, during therapy. Expect drug to be discontinued if patient develops hypertriglyceridemia-induced pancreatitis or triglyceride level exceeds 500 mg/dl.

Monitor diabetic patient’s blood glucose level regularly, as ordered, to assess effectiveness of colesevelam therapy.

When giving colesevelam with a drug that has a narrow therapeutic index, expect to give that drug at least 4 hours before colesevelam to prevent reduced effectiveness.

Because colesevelam may decrease or delay absorption of other , administer it separately if possible. colesevelam hydrochloride 267 C

Make sure that patient drinks enough fluid when taking drug.
WARNING Monitor patients with preexisting constipation, who are at increased risk for developing fecal impaction.

Monitor frequency of bowel movements and consistency of stools in patients with coronary artery disease or hemorrhoids because constipation may aggravate these conditions.

PATIENT SAFTY

Instruct patient to take drug with meals and drink plenty of liquids when taking it.

Tell patient to protect tablets from moisture.

Caution patient against changing prescribed dosage or stopping colesevelam abruptly because serum lipid level may increase significantly.

Remind patient that drug therapy doesn’t reduce the need for dietary changes.

Urge patient to keep regularly scheduled appointments for follow-up blood tests.

Instruct patient to take vitamin supplements at least 4 hours before colesevelam.

Category

Chemical class: Diethylenetriamine and 1chloro-2,3-epoxypropane copolymer, highmolecular-weight anion exchange resin
Therapeutic class: Antihyperlipidemic

Pregnancy category: Not rated

Indications

To treat primary hypercholesterolemia GRANULES
Adults.15 to 30 g daily in divided doses b.i.d. to q.i.d., before meals and at bedtime.
Adults. Initial: 2 g once daily or in divided doses b.i.d., increased every 1 to 2 mo in 2-g increments once or twice daily. Maximum: 16 g daily.

Mechanism of Action

Combines with bile acids in the intestine, preventing their absorption and forming an insoluble complex that’s excreted in feces. Loss of bile acids increases hepatic production of cholesterol to form new bile acids and increases oxidation of cholesterol to bile acids. Depletion of cholesterol increases hepatic LDL receptor activity, which removes LDLs from the blood.

Contraindications

Complete biliary obstruction, hypersensitivity to colestipol or its components

Interactions

chenodiol, ursodiol: Possibly reduced therapeutic effects of colestipol digitalis glycosides: Possibly increased risk of digitalis toxicity when colestipol is stopped furosemide, sulfonylureas, thyroid hormones: Decreased absorption and therapeutic effects of these oral anticoagulants: Possibly increased or decreased anticoagulant effect penicillin G, propranolol, tetracyclines (oral), thiazide diuretics: Decreased absorption of these vancomycin (oral): Possibly marked decrease in vancomycin antibacterial action vitamins (fat-soluble): Possibly interference with vitamin absorption

Side Efect

CNS: Headache
GI: Abdominal distention and pain, constipation, diarrhea, eructation, esophageal reaction, fecal impaction, heartburn, nausea, vomiting

Cautions

Mix colestipol granules with at least 90 ml of fluid before giving it to prevent accidental inhalation or esophageal distress.

Because colestipol may interact with various , give it on a separate schedule from other when possible.

Make sure patient has adequate fluid intake, and obtain an order for a stool softener or laxative to prevent constipation. To prevent impaction, expect to decrease dosage or discontinue drug if constipation occurs or worsens.

Expect to discontinue drug if no response occurs after 3 months.

Monitor patient’s serum cholesterol level as appropriate, usually at baseline, 4 to 6 weeks after starting therapy, and then every 3 months. Expect to reduce monitoring frequency to every 4 months if colestipol hydrochloride 268 response is adequate.

Be aware that HDL and serum triglyceride levels may increase or remain unchanged during colestipol therapy.

Keep in mind that adverse GI reactions are more common in patients over age 60.

PATIENT SAFTY

To help minimize adverse GI reactions, advise patient to mix granules thoroughly in fluid so they’re completely wet before drinking.

Remind patient that colestipol doesn’t reduce the importance of dietary changes.

Caution patient not to increase or decrease prescribed dosage or to suddenly stop taking drug. Explain that stopping drug abruptly may significantly increase serum lipid levels.

Instruct patient to keep appointments for follow-up blood tests.

Teach patient how to prevent constipation, and advise him to contact prescriber if constipation occurs or worsens.

Category

Chemical class: Polypeptide
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To treat acute or chronic gram-negative infections caused by Enterobacter aerogenes, Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa
I.M.INJECTION,
I.V.INJECTION,
IV:
Adults. 2.5 to 5 mg/kg daily in 2 to 4 divided doses. Maximum: 5 mg/kg/day.
DOSAGE ADJUSTMENT For obese patients, dosage should be based on ideal body weight. For patients with severe renal impairment, dosage reduced to 1.5 mg/kg daily and interval reduced to every 36 hr. For patients with moderate renal impairment, interval shouldn’t exceed twice daily and may need to be once daily or every 36 hr. For patients with mild renal impairment, interval shouldn’t exceed twice daily.

Mechanism of Action

Penetrates into and disrupts bacterial cell membrane, resulting in cell death. Colistimethate is an inactive pro-drug of the bioactive form colistin. Colistin binds to gram-negative bacterial cell membrane phospholipids, increasing cell membrane permeability and causing loss of metabolites essential to bacterial existence.

Contraindications

Hypersensitivity to colistimethate or its components, renal disease

Interactions

aminoglycosides, vancomycin: Increased risk of developing nephrotoxicity curaniform muscle relaxants, such as tubocurarine, decamethonium, ether, gallamine, succinylcholine: Potentiated neuromuscular blocking effect of these sodium cephalothin: Possibly enhanced nephrotoxicity

Side Efect

CNS: Dizziness, fever, paresthesia, slurred speech, tingling of extremities, vertigo
GI: Nausea, pseudomembranous colitis, vomiting
GU: Decreased creatinine clearance and urine output, increased BUN and serum creatinine, nephrotoxicity
MS: Muscle weakness
RESP: Apnea, respiratory distress
SKIN: Pruritus, rash, urticaria

Cautions

Use colistimethate cautiously in patients with impaired renal function.

Reconstitute each 150-mg vial with 2 ml sterile water for injection to yield 75 mg/ ml. During reconstitution, swirl vial gently to avoid frothing.

When giving by I.V. injection, slowly inject half of total daily dose over 3 to 5 minutes and repeat dose 12 hours later, as ordered.

When giving by I.V. infusion, slowly inject half of total daily dose over 3 to 5 minutes. Then add remaining half of total daily dose to an appropriate solution, such as normal saline solution or D5W, with type and amount of solution dictated by patient’s fluid and electrolyte needs. Starting 1 to 2 hours after first dose, slowly infuse remaining drug over 22 to 23 hours. colistimethate sodium 269 C If patient has renal impairment, use a reduced infusion rate. Once the infusion is prepared, use within 24 hours.

Notify prescriber if patient develops neurologic changes (paresthesia, tingling of limbs, pruritus, vertigo, dizziness, slurred speech). Dosage may need to be reduced.
WARNING Monitor patient’s BUN and serum creatinine levels, as ordered. If elevated, notify prescriber because drug may cause nephrotoxicity (usually reversible if drug is stopped) with possible renal shutdown. Toxic levels interfere with nerve transmission at neuromuscular junctions, resulting in apnea and muscle weakness.

Monitor patient receiving drug I.M. because apnea and neuromuscular blockade may occur with this route, especially in patients with impaired renal function. Before giving drug I.M., make sure dose is appropriate for degree of renal function.

Monitor patient’s bowel elimination. If diarrhea develops, obtain stool culture to check for pseudomembranous colitis. If confirmed, expect to stop drug and give fluid, electrolytes, and antibiotics effective against Clostridium difficile.

PATIENT SAFTY

Caution patient to avoid performing hazardous activities, including driving, during colistimethate therapy.

Tell patient to immediately report tingling in her extremities, vertigo, dizziness, generalized pruritus, or slurred speech because dosage may need to be decreased.

Explain need for frequent blood tests during therapy to check kidney function.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and can be serious, requiring prompt treatment.

Category

Chemical class: Arginine vasopressin antagonist (antidiuretic hormone)
Therapeutic class: Aquaretic (sodium/water stabilizer)

Pregnancy category: C

Indications

To treat euvolemic and hypervolemic hyponatremia in hospitalized patients such as may occur in the syndrome of inappropriate antidiuretic hormone, hypothyroidism, adrenal insufficiency, or pulmonary disorders

IV

Adults.Loading dose: 20 mg over 30 minutes followed by 20 mg as a continuous infusion over 24 hours. Additional 20 mg daily may be given by continuous infusion for 1 to 3 days, as needed. Maximum: 40 mg daily with total duration of therapy, including loading dose, not to exceed 4 days. Route Onset Peak Duration I.V. Unknown 24 hr Unknown

Mechanism of Action

Binds with arginine vasopressin V2 receptor sites in collecting ducts of kidneys. By doing so, drug blocks action of arginine vasopressin on V2 receptor, decreases water resorption in collecting ducts, increases excretion of free water (urine output), and increases serum sodium concentration, thus correcting water and sodium imbalance.

Incompatibilities

Don’t mix with lactated Ringer’s solution, normal saline solution, or other .

Contraindications

Hypersensitivity to conivaptan or its components; patients with hypovolemic hyponatremia; use with potent CYP3A4 inhibitors such as clarithromycin, indinavir, itraconazole, ketoconazole, and ritonavir

Interactions

amphotericin B, cisplatin, corticosteroids: Possibly additive hypokalemic effects clarithromycin, indinavir, itraconazole, ketoconazole, ritonavir, and other strong CYP3A4 inhibitors: Increased blood conivaptan level digoxin: Possibly increased digoxin level and risk of digioxin toxicity metabolized by CYP3A4, such as HMG-CoA reductase inhibitors: Possibly increased risk of rhabdomyolysis conivaptan hydrochloride 270

Side Efect

CNS: Confusion, fever, headache, insomnia
CV: Atrial fibrillation, hypertension, hypotension, orthostatic hypotension, peripheral edema
EENT: Dry mouth, oral candidiasis, pharyngeal pain
ENDO: Hyperglycemia, hypoglycemia
GI: Constipation, diarrhea, nausea, thirst, vomiting
GU: Hematuria, pollakiuria, polyuria, UTI
HEME: Anemia
RESP: Pneumonia
SKIN: Erythema, pruritus
Other: Dehydration, hypokalemia, hypomagnesemia, hyponatremia, infusion site reactions (erythema, pain, phlebitis, swelling)

Cautions

Conivaptan shouldn’t be used to treat patients with heart failure.

Use cautiously in patients with hepatic or renal dysfunction because levels remain elevated longer in these patients.

Give drug only through large veins, and change infusion site every 24 hours. Drug may cause serious infusion site reactions even when diluted and infused correctly. Inspect site regularly; change immediately if reactions occur.

Dilute 20-mg (4-ml) loading dose with 100 ml of 5% dextrose injection before administration. Gently invert bag several times to mix thoroughly. Use mixture within 24 hours, infusing over 30 minutes.

Dilute 20-mg (4-ml) or 40-mg (8-ml) continuous infusion dose with 250 ml of D5W before use. Gently invert the bag several times to mix thoroughly. Infuse immediately over 24 hours. If infusion is interrupted for any reason, discard any remaining solution 24 hours after mixing.

Monitor neurologic status and serum sodium level closely during therapy because rapid increase in serum sodium level (more than 12 mEq/L/24 hr) may result in serious neurologic impairment. If serum sodium level rises faster than expected, stop infusion temporarily and notify prescriber. If it keeps rising, expect conivaptan to be discontinued. If hyponatremia persists or recurs and patient has no neurologic abnormalities, drug may be resumed at a reduced rate.

Monitor vital signs, and assess patient regularly for hypovolemia. If patient develops hypovolemia or hypotension while receiving conivaptan, stop infusion, notify prescriber, and provide supportive care, as prescribed. After hypovolemia and hypotension have been corrected, drug may be resumed at a reduced rate.

Store ampules in cardboard container, protected from light, until ready for use.

PATIENT SAFTY

Instruct patient to report any infusion site discomfort immediately.

Tell patient that frequent laboratory tests will be performed to monitor his serum sodium level and volume status.

Category

Chemical class: Glucocorticoid
Therapeutic class: Anti-inflammatory, corticosteroid replacement, immunosuppressant

Pregnancy category: Not rated

Indications

To treat allergic and inflammatory disorders, collagen disorders, congenital adrenal hyperplasia, dermatologic disorders, edema (from systemic lupus erythematosus or nephrotic syndrome), GI disorders, hematologic disorders, multiple sclerosis (acute exacerbations), neoplastic diseases, primary or secondary adrenocortical insufficiency, respiratory disorders, rheumatic disorders, trichinosis with myocardial or neurologic involvement, and tuberculous meningitis Adults and adolescents. Initial: 25 to 300 mg before 9 a.m. daily. Maintenance: Dosage adjusted based on patient response. Children.2.5 to 10 mg/kg daily before 9 a.m. For adrenocortical insufficiency, 0.7 mg/kg/day before 9 a.m.
I.M.INJECTION Adults and adolescents.Initial: 25 to 300 mg daily. Maintenance: Dosage adjusted based on patient response. Children.0.83 to 5 mg/kg every 12 to 24 hr. cortisone acetate 271 C For adrenocortical insufficiency, 0.7 mg/kg daily or every third day, or 0.23 to 0.35 mg/ kg daily. Route Onset Peak Duration P.O. Rapid 2 hr 1.25–1.5 days I.M. Slow 20–48 hr 1.25–1.5 days

Mechanism of Action

Binds to intracellular glucocorticoid receptors and suppresses inflammatory and immune responses by:

inhibiting neutrophil and monocyte accumulation at the inflammation site and suppressing their phagocytic and bactericidal activity

stabilizing lysosomal membranes

suppressing the antigen response of macrophages and helper T cells

inhibiting synthesis of cellular mediators of inflammatory response, such as cytokines, interleukins, and prostaglandins.

Contraindications

Hypersensitivity to cortisone or its components, idiopathic thrombocytopenic purpura (parenteral form), live-virus vaccine administration, systemic fungal infection

Interactions

anticholinesterases: Possibly antagonized anticholinesterase effects in myasthenia gravis barbiturates: Decreased cortisone effectiveness, increased cortisol clearance digitalis glycosides: Possibly digitalis toxicity estrogens, oral contraceptives: Increased cortisone effects and risk of toxicity hydantoins,
rifampin: Increased metabolism and decreased effects of cortisone isoniazid: Decreased blood isoniazid level neuromuscular blockers: Possibly enhanced blockade of neuromuscular blockers, leading to increased or prolonged respiratory depression or apnea oral anticoagulants: Possibly obstructed anticoagulant effects potassium-wasting diuretics: Possibly hypokalemia salicylates: Decreased effectiveness and blood level of salicylates somatrem: Decreased growth-promoting effect

Side Efect

CNS: Ataxia, behavior changes, depression, dizziness, euphoria, fatigue, headache, increased ICP with papilledema, insomnia, lassitude, malaise, mood swings, paresthesia, seizures, steroid psychosis, syncope, vertigo
CV: Arrhythmias (from hypokalemia), fat embolism, heart failure, hypertension, hypotension, thromboembolism, thrombophlebitis
EENT: Exophthalmos, glaucoma, increased intraocular pressure, nystagmus, posterior subcapsular cataracts
ENDO: Adrenal insufficiency during stress, Cushing’s syndrome, diabetes mellitus, growth suppression in children, hyperglycemia, negative nitrogen balance from protein catabolism
GI: Abdominal distention, hiccups, increased appetite, nausea, pancreatitis, peptic ulcer, ulcerative esophagitis, vomiting
GU: Glycosuria, menstrual irregularities, perineal burning or tingling
HEME: Leukocytosis
MS: Arthralgia; aseptic necrosis of femoral and humeral heads; compression fractures; muscle atrophy, weakness, and twitching; myalgia; osteoporosis; spontaneous fractures; steroid myopathy; tendon rupture
SKIN: Acne; diaphoresis; ecchymosis; erythema; hirsutism; hyperpigmentation; hypopigmentation; necrotizing vasculitis; petechiae; purpura; rash; scarring; sterile abscesses; striae; subcutaneous fat atrophy; thin, fragile skin; urticaria
Other: Anaphylaxis, hypocalcemia, hypokalemia, hypokalemic alkalosis, impaired wound healing, masking of infection, metabolic alkalosis, suppressed skin test reaction, weight gain

Cautions

Use cortisone cautiously in patients with ocular herpes simplex because corneal perforation may occur.

Expect prescriber to order baseline ophthalmologic examination before therapy starts because prolonged use of cortisone may result in glaucoma, increased intraocular pressure, and damage to optic nerve.

Assess patient for signs and symptoms of infection before giving cortisone because drug may mask them. Be aware that new cortisone acetate 272 infections may develop during therapy because of risk of immunosuppression. If a new infection develops, expect to administer appropriate antibiotics.

Obtain serum electrolyte levels before therapy, as ordered, and monitor results often during therapy to detect electrolyte imbalances. Increased calcium excretion, potassium depletion, and sodium and water retention may occur with large doses of cortisone. Anticipate the need for potassium and calcium supplementation and sodium restriction, if indicated.

Keep in mind that prescriber will order lowest effective dose.

To avoid peptic ulcer formation from cortisone, expect patient to receive concurrent antacid or antihistamine therapy.
WARNING Be aware that live-virus vaccines shouldn’t be given during cortisone therapy because patient may become immunosuppressed and develop the viral infection.
WARNING Assess for adrenal suppression or insufficiency (fatigue, hypotension, lassitude, nausea, vomiting, and weakness) in patient exposed to stress or receiving prolonged cortisone therapy. Notify prescriber immediately if patient has evidence of this life-threatening adverse reaction.

Watch for signs and symptoms of steroid psychosis (confusion, delirium, euphoria, insomnia, mood swings, personality changes, severe depression), which may develop 15 to 30 days after starting drug. Be prepared to stop drug if such signs occur. If stopping isn’t possible, expect to administer a psychotropic drug.

Watch for cushingoid signs, such as acne, buffalo hump, central obesity, ecchymosis, moon face, striae, and weight gain. Notify prescriber at once if they occur.

Expect to taper oral cortisone dosage slowly to prevent withdrawal syndrome (abdominal or back pain, anorexia, dizziness, fever, headache, and syncope).

PATIENT SAFTY

Instruct patient to take oral cortisone exactly as prescribed, every morning before 9 a.m. Advise him to take it with food if GI distress occurs.

Caution patient not to stop drug abruptly because doing so may lead to adrenal insufficiency, withdrawal symptoms, or both.

Inform patient about adrenal insufficiency and need for possible dosage increases during stress. Advise him to notify prescriber immediately if signs or symptoms develop or if he’s exposed to stress.

Caution patient to avoid exposure to people with infections because cortisone can cause immunosuppression. Also, teach him to recognize and immediately report signs and symptoms of infection.

Teach patient to recognize and report

Side Efect

, including Cushing’s syndrome.

Urge patient receiving long-term cortisone therapy to carry medical identification.

Recommend regular eye examinations.

Urge patient to keep follow-up appointments with prescriber, which may include laboratory tests, to evaluate effects of therapy.

Category

Chemical class: Disodium chromoglycate
Therapeutic class: Antiasthmatic, antiinflammatory

Pregnancy category: B

Indications

To prevent bronchial asthma attacks AEROSOL(METERED-DOSE INHALER) Adults and children over age 5. 2 metered sprays (1.6 to 2 mg) every 4 to 6 hr. Maximum: 16 sprays (12.8 to 16 mg) daily. FOR INHALATION Adults and children over age 2. 1 capsule (20 mg) every 4 to 6 hr. Maximum: 8 capsules (160 mg) daily. SOLUTION FOR NEBULIZATION Adults and children over age 2. 20 mg every 4 to 6 hr. Maximum: 160 mg daily. To prevent bronchospasm caused by environmental exposure or exercise AEROSOL(METERED-DOSE INHALER) Adults and children over age 5. 2 metered cromolyn sodium 273 C sprays (1.6 to 2 mg) as a single dose at least 10 to 15 min (no longer than 1 hr) before exposure or exercise. Maximum: 16 sprays (12.8 to 16 mg) daily. FOR INHALATION Adults and children over age 2. 1 capsule (20 mg) as single dose inhaled at least 10 to 15 min (no longer than 1 hr) before exposure or exercise. Maximum: 8 capsules (160 mg) daily. SOLUTION FOR NEBULIZATION Adults and children over age 2. Initial: 20 mg inhaled 10 to 15 min (no longer than 1 hr) before exposure or exercise. Repeated p.r.n. during prolonged exercise. Maximum: 160 mg daily. To treat allergic rhinitis NASAL SOLUTION Adults and children over age 2. 1 spray (5.2 mg) in each nostril at regular intervals t.i.d. or q.i.d. Maximum: 1 spray (5.2 mg) in each nostril 6 times daily. To prevent systemic mastocytosis , ORAL CONCENTRATE Adults and adolescents.200 mg q.i.d., 30 min before meals and at bedtime. Children ages 2 to 12. 100 mg q.i.d., 30 min before meals and at bedtime. Maximum: 40 mg/kg/day. Children under age 2. 5 mg/kg q.i.d. Maximum: 40 mg/kg daily.

Contraindications

Arrhythmias, coronary artery disease (aerosol); hypersensitivity to cromolyn or its components, status asthmaticus (all forms); nasal polyps (nasal solution) Route Onset Peak Duration Aerosol Minutes Unknown Up to 2 hr Nasal 1 wk 1–4 wk Unknown solution Nebulizer Minutes Unknown 3–6 hr solution

Side Efect

CNS: Dizziness, headache, neuritis
EENT: Burning eyes, hoarseness, laryngeal edema, nasal congestion, and swollen parotid glands (all forms); increased sneezing, nasal stinging, and throat irritation (nasal solution); taste perversion (aerosol)
GI: Anorexia, diarrhea (capsules and oral concentrate), nausea, vomiting
GU: Dysuria, urinary frequency
MS: Arthralgia, joint swelling
RESP: Cough, wheezing
SKIN: Rash, urticaria

Cautions

WARNING Be aware that cromolyn sodium shouldn’t be used to relieve acute asthma attack or severe bronchospasm; it should be used only for prevention.

Don’t give cromolyn sodium through handheld nebulizer. Instead, administer via power-operated nebulizer with a face mask or mouthpiece.

Evaluate patient for effective inhalation; patient must be able to inhale adequately for nebulizer solution to be effective. Antigen IgE antibody Nucleus Granule Mast cell Degranulation Degranula- tion blocked by cromolyn 1 2 3

Mechanism of Action

In asthma, inflammation results when antigen reexposure causes mast cells to degranulate and release histamine and chemical mediators. Cromolyn helps reduce inflammation by preventing degranulation.After exposure to an antigen, mast cells become sensitized to it and immunoglobulin E (IgE) antibodies appear on their surfaces.When the antigen returns, it attaches to IgE (1 in the illustration) and triggers events that lead to degranulation (2). By preventing granules from opening on the cells’surfaces (3), cromolyn blocks release of histamine and chemical mediators.

Thoroughly mix oral concentrate or capsule contents into half a glass of hot water (not fruit juice, milk, or food), and let cool before administering.

Give drug at regular intervals to maximize effectiveness.

PATIENT SAFTY

Teach patient how to use power-operated nebulizer; warn against using handheld nebulizer.

Advise patient to use cromolyn sodium 10 to 15 minutes before exercising or exposure to other precipitating factors.

Instruct patient to thoroughly mix oral concentrate with hot water (not fruit juice, milk, or food) and let it cool before drinking.

Inform patient that
NASAL SPRAY may cause minor nasal irritation.

Explain that cromolyn sodium may take up to 1 month to reach full therapeutic effects.

Category

Chemical class: Synthetic chloroformate salt
Therapeutic class: Antipruritic, scabicide

Pregnancy category: C

Indications

To treat scabies CREAM, LOTION
Adults. 30 to 60 g (thin layer) massaged into skin from chin down and repeated in 24 hr. Applied p.r.n. to skin folds, creases, and areas of intense pruritus for up to 48 hr. To relieve pruritus caused by scabies CREAM, LOTION
Adults.30 to 60 g (thin layer) massaged gently into affected areas until drug is completely absorbed. Repeated p.r.n.

Mechanism of Action

Exerts a toxic effect on Sarcoptes scabiei by an unknown mechanism.

Contraindications

Abrasions, application to mucous membranes, breaks in skin, hypersensitivity to crotamiton or its components, inflammation

Side Efect

SKIN: Contact dermatitis, irritation, pruritus, rash

Cautions

Expect pruritus to continue for 4 to 6 weeks after treatment.

PATIENT SAFTY

Advise patient to shake lotion bottle well before applying.

Warn him to keep drug away from eyes, nose, mouth, and inflamed skin.

Advise patient to use a topical corticosteroid for dermatitis and an antihistamine for pruritus, as prescribed.

Instruct patient to change clothing and bed linens the morning after final application and to take a cleansing bath 48 hours after final application.

Inform patient that pruritus may continue for 4 to 6 weeks after treatment.

Advise patient to notify prescriber if skin irritation or rash occurs.

Category

Chemical class: Piperazine derivative
Therapeutic class: Anticholinergic, antiemetic

Pregnancy category: B

Indications

To prevent postoperative vomiting
I.M.INJECTION Adults and adolescents.50 mg 15 to 30 min before surgery ends; then every 4 to 6 hr, p.r.n., for first few postoperative days. Children ages 6 to 12. 25 mg 15 to 30 min before surgery ends; then t.i.d., p.r.n., for first few postoperative days. Children up to age 6. 12.5 mg 15 to 30 min before surgery ends; then t.i.d., p.r.n., for first few postoperative days. To prevent and treat motion sickness Adults and adolescents.50 mg 30 min crotamiton;cyclizine 275 C before travel; then every 4 to 6 hr, p.r.n. Maximum: 200 mg daily. Children ages 6 to 12. 25 mg 30 min before travel; then every 6 to 8 hr, p.r.n. Maximum: 75 mg daily.
I.M.INJECTION Adults and adolescents. 50 mg every 4 to 6 hr, p.r.n. Children.1 mg/kg t.i.d., p.r.n. Route Onset Peak Duration P.O., I.M. 30–60 min Unknown 4–6 hr

Mechanism of Action

May act centrally on the vomiting center by blocking chemoreceptor trigger zones. Cyclizine also may reduce the sensitivity of the labyrinthine apparatus in the inner ear.

Contraindications

Hypersensitivity to cyclizine or its components, shock

Interactions

anticholinergics: Possibly potentiated anticholinergic effects apomorphine: Possibly decreased emetic response of apomorphine
CNS depressants: Possibly potentiated CNS depression
alcohol use: Possibly potentiated CNS depression

Side Efect

CNS: Dizziness, drowsiness, euphoria, excitation, hallucinations, insomnia, nervousness, restlessness, seizures (in children), vertigo
CV: Hypotension, palpitations, tachycardia
EENT: Blurred vision; diplopia; dry mouth, nose, and throat; tinnitus
GI: Anorexia, constipation, diarrhea, nausea, vomiting
GU: Urinary frequency and hesitancy, urine retention
SKIN: Jaundice, rash, urticaria

Cautions

Help patient with ambulation, and take safety precautions to prevent injury from falls if drowsiness or dizziness occurs.

Don’t schedule allergen skin tests until at least 5 days after stopping cyclizine; drug may interfere with test results.

PATIENT SAFTY

Urge patient to avoid alcohol and other CNS depressants during cyclizine therapy.

Advise patient to ask for help with ambulation if he feels drowsy or dizzy.

Category

Chemical class: Tricyclic amine salt
Therapeutic class: Skeletal muscle relaxant

Pregnancy category: B

Indications

As adjunct to rest and physical therapy for relief of muscle spasm associated with acute, painful musculoskeletal conditions Adults and adolescents.5 mg t.i.d., increased as needed to 10 mg t.i.d. Maximum: 30 mg daily for 3 wk.
DOSAGE ADJUSTMENT Dosage frequency reduced in elderly patients and those with hepatic impairment. Route Onset Peak Duration P.O. 1 hr 1–2 wk 12–24 hr

Mechanism of Action

Acts in the brain stem to reduce or abolish tonic muscle hyperactivity. Because cyclobenzaprine doesn’t act at the neuromuscular junction or directly on skeletal muscle, it relieves muscle spasm without disrupting muscle function.

Contraindications

Acute recovery phase of MI; age less than 12; arrhythmias, including heart block and other conduction disturbances; heart failure; hypersensitivity to cyclobenzaprine or its components; hyperthyroidism; MAO inhibitor use within 14 days

Interactions

anticholinergics, antidyskinetics: Possibly potentiated anticholinergic effects of these CNS depressants, tricyclic antidepressants: cyclobenzaprine hydrochloride 276 Possibly additive CNS depressant effects of these , increased risk of adverse effects of antidepressants and cyclobenzaprine guanadrel, guanethidine: Possibly decreased or blocked antihypertensive effects of these
MAO inhibitors: Possibly hyperpyretic crisis, severe seizures, and death
alcohol use: Possibly additive CNS depression

Side Efect

CNS: Asthenia, confusion, depression, dizziness, drowsiness, fatigue, fever, headache, insomnia, irritability, nervousness, paresthesia, seizures, tremor, weakness
CV: Arrhythmias, including tachycardia; orthostatic hypotension; palpitations; vasodilation
EENT: Blurred vision, diplopia, dry mouth, transient vision loss, unpleasant taste
GI: Constipation, hiccups, indigestion, nausea, vomiting
GU: Libido changes, urinary frequency, urine retention
SKIN: Diaphoresis, facial flushing, pruritus, rash

Cautions

Use cyclobenzaprine cautiously in patients with history of low seizure threshold.

If possible, avoid giving drug to elderly patients because of its anticholinergic effects.

To prevent falls, take safety precautions if patient is confused, dizzy, or weak.

PATIENT SAFTY

Urge patient to avoid alcohol and other CNS depressants during therapy.

Inform patient about possible lack of alertness and dexterity.

Advise patient to ask for assistance with walking, driving, or hazardous activities if he experiences dizziness or weakness.

Category

Chemical class: D-alanine analogue, Streptomyces garyphalus or Streptomyces orchidaceus derivative
Therapeutic class: Antitubercular

Pregnancy category: C

Indications

To treat tuberculosis with other antituberculotics after failure of primary , including ethambutol, isoniazid, pyrazinamide, rifampin, streptomycin Adults and adolescents. 250 mg every 12 hr for 2 wk; then every 6 to 8 hr for 2 wk. Dosage increased gradually to maintain blood cycloserine level below 30 mcg/ ml. Maximum: 1 g daily. Children. 10 to 20 mg/kg daily in divided doses every 12 hr. Maximum: 1 g daily.

Mechanism of Action

Inhibits bacterial cell wall synthesis in gram-positive organisms, including Mycobacterium tuberculosis. In early stages of bacterial cell wall synthesis, cycloserine inhibits two enzymes that help form peptidoglycan, which is needed to make the cell membrane rigid and protective.

Contraindications

Chronic alcoholism, depression, hypersensitivity to cycloserine or its components, psychosis, renal disease, seizure disorder, severe anxiety

Interactions

ethionamide: Possibly increased risk of seizures isoniazid: Possibly increased risk of adverse CNS effects
phenytoin: Possibly increased blood phenytoin level pyridoxine: Possibly anemia or peripheral neuritis
alcohol use: Possibly increased risk of seizures

Side Efect

CNS: Aggression, anxiety, coma, confusion, depression, dizziness, drowsiness, headache, irritability, lethargy, memory loss, nervousness, nightmares, psychosis, restlessness, seizures, suicidal tendencies, tremor, vertigo
CV: Heart failure
HEME: Leukocytosis, megaloblastic anemia
MS: Dysarthria, hyperreflexia
SKIN: Dermatitis, photosensitivity cycloserine 277 C
Other: Folic acid deficiency, vitamin B12 deficiency

Cautions

Monitor blood cycloserine level, as appropriate. Blood level should be maintained at 25 to 30 mcg/ml.

Monitor mental status, mood, and affect for aggression or depression.

Monitor CBC to detect blood dyscrasias.

To prevent injury from falls, take safety precautions if adverse CNS reactions, such as dizziness or drowsiness, develop.

PATIENT SAFTY

Urge patient to avoid alcohol while taking cycloserine.

Instruct patient to seek help immediately if he has suicidal thoughts.

Advise patient to avoid driving and to ask for assistance with walking or hazardous activities if he develops adverse CNS reactions, such as dizziness and drowsiness.

Tell patient to contact prescriber if symptoms haven’t improved after 2 to 3 weeks.

Emphasize the importance of complying with drug therapy because effective treatment may take years to complete.

Category

Chemical class: Tolypocladium inflatum Gams– or Cylindrocarpon lucidum Booth–derived polypeptide
Therapeutic class: Antipsoriatic, antirheumatic, immunosuppressant

Pregnancy category: C

Indications

To prevent or treat organ rejection in kidney, liver, and heart allogenic transplantation , MODIFIED , MODIFIED ORAL SOLUTION, Adults and children.Initial: 12 to 15 mg/kg daily in divided doses every 12 hr starting 4 to 12 hr before surgery and continuing 1 to 2 wk afterward. Then, dosage reduced by 5% every wk to maintenance dose. Maintenance: 5 to 10 mg/kg daily in divided doses every 12 hr.

IV

Adults.2 to 6 mg/kg daily starting 4 to 12 hr before surgery and continuing afterward until patient can tolerate oral form of drug. To treat severe rheumatoid arthritis MODIFIED , MODIFIED
Adults. 2.5 mg/kg daily in divided doses every 12 hr, increased by 0.5 to 0.75 mg/kg daily after 8 wk and again after 12 wk. Maximum: 4 mg/kg daily. To treat psoriasis MODIFIED , MODIFIED
Adults.Initial: 2.5 mg/kg daily in divided doses b.i.d., increased by 0.5 mg/kg daily after 4 wk. Then dosage increased every 2 wk, if needed. Maximum: 4 mg/kg daily.

Mechanism of Action

Causes immunosuppression by inhibiting the proliferation of T lymphocytes, the production and release of lymphokines, and the release of interleukin-2.

Contraindications

Abnormal renal function, neoplastic diseases, and uncontrolled hypertension in patients with psoriasis or rheumatoid arthritis (modified capsules and oral solution); hypersensitivity to cyclosporine, its components, or polyoxyethylated castor oil (I.V. infusion)

Interactions

ACE inhibitors, angiotensin II receptor antagonists, potassium-sparing diuretics, potassium supplements: Increased risk of hyperkalemia allopurinol, amiodarone, azithromycin, bromocriptine, clarithromycin, colchicine, danazol, diltiazem, erythromycin, fluconazole, hormonal contraceptives, imatinib, itraconazole, ketoconazole, methylprednisolone, metoclopromide, nefazodone, nicardipine, oral contraceptives, quinupristin and dalfopristin, verapamil, voriconazole: Increased cyclosporine level amphotericin B, azapropazon, cimetidine, ciprofloxacin, colchicine, co-trimoxazole, fibric acid derivatives (bezafibrate, fenofibrate), gentamicin, ketoconazole, melphalan, NSAIDs, ranitidine, tacrolimus, tobramycin, vancomycin: Increased risk of nephrotoxicity atorvastatin, fluvastatin, lovastatin, pravastatin, simvastatin: Risk of myotoxicity cyclosporine 278 bosentan, carbamazepine, nafcillin, octreotide, orlistat, oxcarbazepine, phenobarbital, phenytoin, rifampin, St. John’s wort, sulfinpyrazone, terbinafine, ticlopidine: Decreased blood cyclosporine level and therapeutic response colchicine: Possibly colchicine toxicity, such as myopathy and neuropathy digoxin: Increased blood digoxin level and risk of digitalis toxicity indinavir, nelfinavir, ritonavir, saquinavir: Possibly increased blood cyclosporine level methotrexate: Increased blood methotrexate level and risk of renal dysfunction methylprednisolone (high dose): Increased risk of seizures other immunosuppressants: Possibly excessive immunosuppression prednisolone: Increased prednisolone level repaglinide: Possibly increased repaglinide level and risk of hypoglycemia sirolimus: Increased blood sirolimus level vaccines (killed or live virus): Possibly suppressed immune response and increased adverse effects of vaccine Grapefruit, grapefruit juice: Increased risk of nephrotoxicity Potassium-rich : Increased risk of hyperkalemia

Side Efect

CNS: Altered level of consciousness, confusion, headache, intracranial hypertension, loss of motor function, paresthesia, psychiatric disturbances, seizures, tremor
CV: Chest pain, hypertension
EENT: Gingival hyperplasia, optic disc edema, oral candidiasis, visual impairment
ENDO: Gynecomastia
GI: Diarrhea, nausea, pancreatitis, vomiting
GU: Albuminuria, hematuria, nephropathy associated with BK virus, proteinuria, renal failure
HEME: Anemia, leukopenia, thrombocytopenia
SKIN: Acne, cancer, flushing, hirsutism, rash
Other: Anaphylaxis, hyperkalemia, hypomagnesemia, life-threatening infections, lymphoma and other malignancies

Cautions

Be aware that capsules and oral solution aren’t interchangeable with modified capsules and modified oral solution. Modified forms have greater bioavailability.

Prepare I.V. infusion by diluting each milliliter of concentrate in 20 to 100 ml of normal saline solution or D5W. Use glass containers because of possible leaching of diethylhexyphthalate from polyvinyl chloride bags into cyclosporine solution.

Administer I.V. infusion over 2 to 6 hr. If needed, drug may be infused over 24 hr.
WARNING Closely monitor patient for anaphylaxis, at least during first 30 minutes of I.V. administration. Make sure emergency equipment and are immediately available.
WARNING Be aware that rapid I.V. infusion may cause acute nephrotoxicity.

Don’t draw blood to measure cyclosporine level through same I.V. tubing used to administer drug, even if line was flushed after administration. Blood level may be falsely elevated.

Discard diluted solution after 24 hours.

Be aware that oral solution contains alcohol and shouldn’t be administered to patient who drinks heavily or has a history of alcohol dependence.

Don’t add water to oral solution because it will alter drug’s effectiveness.

Avoid giving oral cyclosporine with grapefruit juice, which may raise trough level, increasing risk of nephrotoxicity.

Monitor blood pressure, especially in patients with a history of hypertension, because drug can worsen this condition. Expect to decrease dosage if hypertension develops.

Monitor liver and renal function tests, as ordered, to detect decreased function.

Although uncommon, cyclosporine may cause neurotoxicity, especially after liver transplantation. Watch for evidence of encephalopathy (impaired consciousness, loss of motor function, psychiatric disurbance, seizures, visual disturbance).

Be aware that cyclosporine use may result in increased serum cholesterol levels.

Be aware that St. John’s wort may decrease blood cyclosporine level.

Store capsules at 77° F (25° C) in prepackaged foil wrap to protect them from light.

Expect about 50% of patients treated for psoriasis to relapse about 4 months after therapy stops. cyclosporine 279 C
WARNING Watch for evidence of infection (such as fever, pain, cough, malaise) because patients receiving immunosuppressants such as cyclosporine are at increased risk for viral, bacterial, fungal, and parasitic infection. Watch for both generalized and localized infections, including worsening of pre-existing infections, and be aware that these infections may become life-threatening. Activation of latent viral infections may also occur and include BK virus–associated nephropathy that can lead to decreased renal function and renal graft loss.

PATIENT SAFTY

Instruct patient to take drug at same time each day and in same relation to type and timing of food intake to help increase compliance and maintain steady blood level.

Advise patient to mix oral solution in a glass—not plastic—container with roomtemperature orange or apple juice to improve flavor. Caution him to avoid grapefruit juice because it alters drug metabolism.

Instruct patient to use syringe supplied by manufacturer to ensure accurate measurement of oral solution dose and to wipe— not rinse—syringe after use to prevent cloudiness.

Advise patient not to stop taking drug without consulting prescriber.

Instruct patient to avoid virus vaccines during therapy and people who have received such vaccines. Or, suggest wearing a protective mask when he’s around them.

Caution patient to avoid people who have infections during therapy because cyclosporine causes immunosuppression.

Advise good dental hygiene because of risk of gingival hyperplasia.

Advise patient to discard oral solution after it has been opened for 2 months.

Inform patient with rheumatoid arthritis that drug effects may not appear for 4 to 6 weeks.

Caution patient to avoid excessive exposure to ultraviolet light.

Category

Chemical class: Monoclonal antibody
Therapeutic class: Immunosuppressant

Pregnancy category: C

Indications

To prevent acute organ rejection after kidney transplantation
IV: Adults and children. 1 mg/kg given in five doses. Dose 1 given no more than 24 hr before transplantation; doses 2 through 5 given at 14-day intervals.

Mechanism of Action

Inhibits interleukin-2–mediated activation of lymphocytes, which prevents WBCs from attacking the transplanted kidney. Drug also reduces the body’s infection-fighting ability.

Contraindications

Hypersensitivity to daclizumab or its components

Side Efect

CNS: Anxiety, chills, depression, dizziness, fatigue, fever, headache, insomnia, prickly sensation, tremor, weakness
CV: Chest pain, edema, hypertension, hypotension, tachycardia, thrombosis
EENT: Blurred vision, pharyngitis, rhinitis
ENDO: Hyperglycemia
GI: Abdominal distention and pain, constipation, diarrhea, flatulence, gastritis, heartburn, hemorrhoids, indigestion, nausea, vomiting
GU: Dysuria, hematuria, hydronephrosis, oliguria, renal insufficiency, renal tubular necrosis, urine retention
HEME: Bleeding
MS: Arthralgia, back pain, leg cramps, myalgia
RESP: Atelectasis, cough, crackles, dyspnea, hypoxia, lung congestion, pleural effusion, pulmonary edema
SKIN: Acne, diaphoresis, hirsutism, impaired wound healing, night sweats, pruritus, rash
Other: Dehydration, fluid overload, injection site pain and redness, lymphocele

Cautions

Dilute calculated dose of daclizumab in 50 ml of normal saline solution. Gently invert bag to mix. To prevent foaming, don’t shake it.

Use room temperature solution within 4 hours or refrigerate it for up to 24 hours. Discard unused solution.

Because daclizumab’s compatibility with other isn’t known, don’t add or simultaneously infuse other through same I.V. line.

Monitor blood glucose level for increases during therapy.
WARNING Although daclizumab seldom causes severe hypersensitivity reactions, keep to treat such a reaction nearby for immediate use.

PATIENT SAFTY

Urge patient to complete the course of therapy and return for follow-up visits.

Category

Chemical: Aminopyridine Therapeutic: Potassium channel blocker

Pregnancy category: C

Indications

To improve walking in patients with multiple sclerosis
Adults. 10 mg twice daily Route Onset Peak Duration P.O. 1–2 hr 3–4 hr 10–11 hr

Mechanism of Action

May improve walking in multiple sclerosis patients by blocking potassium channels. When potassium channels are blocked, there is increased conduction of action potentials in demyelinated axons resulting in improved muscle action. D

Contraindications

History of seizures, hypersensitivity to dalfampridine or its components, moderate or severe renal impairment (creatinine clearance of 50 ml/min/1.73 m2or less)

Interactions

other aminopyridine agents: Increased risk of

Side Efect

Side Efect

CNS: Asthenia, balance disorder, confusion, dizziness, headache, insomnia, paresthesia, seizures
EENT: Nasopharyngitis, pharyngolaryngeal pain
GI: Constipation, dyspepsia, nausea
GU: UTI
MS: Back pain, multiple sclerosis relapse

Cautions

Check patient’s creatinine clearance, as ordered, before starting dalfampridine.

Use dalfampridine cautiously in patients with mild renal failure (creatinine clearance 51 to 80 ml/min/1.73 m2) because seizures may occur. If they do, expect drug to be discontinued.

Drug shouldn’t be taken with compounded 4-AP, 4-aminopyridine, or fampridine because the risk of seizures may increase.

Monitor patient’s ability to walk to determine drug’s effectiveness.

PATIENT SAFTY

Tell patient to space dalfampridine doses about 12 hours apart.

Instruct patient, especially one with mild renal impairment, to notify prescriber and stop dalfampridine if seizures occur.

Review signs and symptoms of UTI (pain on urination, frequency or urgency with urination, cloudy appearance to urine) and tell patient to report any such effects to the prescriber.

Category

Chemical class: Low-molecular-weight heparin
Therapeutic class: Anticoagulant, antithrombotic

Pregnancy category: B

Indications

To prevent ischemic complications in patients who receive aspirin as part of treatment for unstable angina and non–Q-wave MI SUBCUTANEOUS INJECTION
Adults.120 international units/kg every 12 hr with aspirin (75 to 165 mg daily) until patient is stable, usually 5 to 8 days. Maximum: 10,000 international units/dose. To prevent blood clots in patients undergoing hip replacement surgery SUBCUTANEOUS INJECTION
Adults. Initial: 2,500 international units 1 to 2 hr before surgery, repeated in 8 to 12 hr and again 8 to 12 hr later. Maintenance: 5,000 international units every morning for 5 to 10 days postoperatively or until patient is fully ambulatory. Alternate: 5,000 international units the evening before surgery; then 5,000 international units daily (starting the next evening) for 5 to 10 days or until patient is fully ambulatory. To prevent blood clots in patients undergoing abdominal surgery who are at risk for thromboembolic complications SUBCUTANEOUS INJECTION
Adults.2,500 international units daily, starting 1 to 2 hr before surgery and repeated for 5 to 10 days. For patients at high risk (those with cancer), 5,000 international units the evening before surgery, repeated daily for 5 to 10 days; or 2,500 international units 1 to 2 hr before surgery followed by 2,500 international units 12 hr later and then 5,000 international units daily for 5 to 10 days. To prevent blood clots in patients with severe mobility restrictions during acute illness SUBCUTANEOUS INJECTION
Adults. 5,000 international units daily. To treat symptomatic venous thromboembolism and prevent recurrence in patients with cancer SUBCUTANEOUS INJECTION
Adults. 200 international units/kg (not to exceed 18,000 international units) once daily for 30 days. Then 150 international units/kg once daily for 5 more mo. dalteparin sodium 282

Mechanism of Action

Binds to and accelerates the activity of antithrombin III, thus inhibiting thrombin and blocking the formation of fibrin clots.

Incompatibilities

Don’t mix dalteparin with other .

Contraindications

Active major bleeding; hypersensitivity to low-molecular-weight heparins, heparin, or pork products; thrombocytopenia associated with positive tests for antiplatelet antibodies in the presence of dalteparin

Interactions

NSAIDs, oral anticoagulants, platelet aggregation inhibitors, thrombolytics: Possibly increased risk of hemorrhage and spinal or epidural hematoma

Side Efect

GI: Elevated liver emzymes
HEME: Hemorrhage, thrombocytopenia
SKIN: Alopecia, bullous eruption, necrosis, pruritus, rash
Other: Anaphylaxis, injection site hematoma and pain

Cautions

Use dalteparin with extreme caution in patients with a history of heparin-induced thrombocytopenia; those at increased risk for hemorrhage (such as those who use a platelet inhibitor or have bacterial endocarditis, bleeding disorders, active ulcerative GI disease, uncontrolled hypertension, or hemorrhagic stroke); and those with recent brain, eye, or spinal surgery.

Use drug cautiously in patients with bleeding diathesis, diabetic retinopathy, platelet defects, recent GI bleeding, severe hepatic or renal insufficiency, or thrombocytopenia.

Before giving first dose, tell Jewish or Islamic patients that drug comes from porcine intestine.

Risk factors for thromboembolic events include age over 40, cancer, history of deep vein thrombosis or pulmonary embolism, obesity, and planned use of anesthesia for more than 30 minutes.

Don’t give drug by I.M. or I.V. injection.

With patient seated or supine, administer drug deep into subcutaneous tissue in Ushaped area around navel, upper outer thigh, or upper outer quadrant of buttocks. If using area around navel or on thigh, lift skin fold with thumb and forefinger while giving injection. Insert entire length of needle at a 45to 90-degree angle. Rotate sites daily.

Routine coagulation tests and dosage adjustments usually aren’t required.
WARNING Monitor patient receiving dalteparin and epidural or spinal anesthesia or spinal puncture because spinal hematomas can occur, causing long-term or permanent paralysis. Watch for evidence of neurologic impairment, such as changes in sensory or motor function. If present, notify prescriber immediately; patient needs urgent care to minimize effect of hematoma. Use of indwelling epidural catheters, concurrent use of other that affect hemostasis, a history of traumatic or repeated epidural or spinal punctures, or a history of spinal deformity or spinal surgery increases the risk of spinal or epidural hematoma in patients receiving dalteparin.

PATIENT SAFTY

If therapy will continue at home, teach patient or caregiver to select injeciton sites, give subcutaneous injections, and rotate sites daily. Tell patient to discard drug if it’s discolored or contains particles. Review safe handling and disposal of syringes and needles.

Teach patient to store drug at room temperature, away from moisture and heat.

Urge patient to report

Side Efect

, especially bleeding, and to seek help immediately if signs of thromboembolism develop, such as severe dyspnea (pulmonary embolism) or neurologic deficits (cerebral embolism).

Stress the importance of follow-up visits.

Category

Chemical class: Glycosaminoglycan heparinoid, low-molecular-weight heparin
Therapeutic class: Anticoagulant, antithrombotic

Pregnancy category: B

danaparoid sodium 283 D

Indications

To prevent deep vein thrombosis after hip replacement surgery SUBCUTANEOUS INJECTION
Adults. 750 anti-factor Xa units b.i.d. (first dose 1 to 4 hr preoperatively; second dose no sooner than 2 hr after surgery) for 7 to 14 days, as indicated.

Mechanism of Action

Inhibits thrombin generation in coagulation pathway, thus preventing fibrin formation and clotting.

Contraindications

Active major bleeding (including hemorrhagic stroke);hypersensitivity to low-molecularweight heparins,heparin,or pork products; severe hemorrhagic disorders,such as hemophilia and thrombocytopenic purpura;sulfite sensitivity;type II thrombocytopenia associated with positive laboratory tests for antiplatelet antibodies in the presence of danaparoid

Interactions

NSAIDs, oral anticoagulants, platelet aggregation inhibitors: Possibly increased risk of bleeding

Side Efect

CNS: Asthenia, dizziness, fever, headache, insomnia
CV: Chest pain, edema
GI: Abdominal pain, constipation, nausea, vomiting
GU: Urine retention, UTI
HEME: Anemia, excessive bleeding
MS: Arthralgia, myalgia
SKIN: Pruritus, rash
Other: Anaphylaxis, injection site pain

Cautions

Use danaparoid with extreme caution in patients at increased risk for hemorrhage (such as those with severe uncontrolled hypertension, acute bacterial endocarditis, bleeding disorders, active ulcerative GI disease, severe renal dysfunction, or nonhemorrhagic stroke); those with a postoperative indwelling epidural catheter; and those with recent had brain, eye, or spinal surgery.

Before administering first dose, inform Jewish and Islamic patients that drug comes from porcine intestinal mucosa.

Don’t give drug by I.M. or I.V. injection.

Administer drug with patient lying down. Use a 25G or 26G needle to minimize tissue trauma. Select site on left or right anterolateral or posterolateral abdominal wall. Hold skin fold gently between thumb and forefinger, and insert entire length of needle deep into subcutaneous tissue at a 45to 90-degree angle. Don’t pinch or rub site afterward. Rotate sites.

Expect to monitor results of CBC and fecal occult blood tests during therapy. Typical coagulation tests, such as PT, APTT, clotting time, whole blood clotting time, and thrombin time, aren’t useful for monitoring drug’s anticoagulant effect.

PATIENT SAFTY

If therapy must continue at home, teach patient or caregiver how to give subcutaneous injections. Review injection sites, and instruct her to rotate them daily. Tell her to discard drug if it’s discolored or contains particles. Review safe handling and disposal of syringes and needles.

Teach patient to store drug at room temperature, away from moisture and heat.

Instruct patient to consult prescriber before using aspirin, ibuprofen, indomethacin, ketoprofen, naproxen, and other NSAIDs because they may increase the risk of bleeding.

Advise patient to stop taking drug and seek help immediately if she experiences severe dizziness, fever, rash, wheezing, or prolonged or unexplained bleeding and pain at the injection site.

Category

Chemical class: Hydantoin derivative, imidazolidinedione sodium salt
Therapeutic class: Antispastic, malignant hyperthermia therapy adjunct

Pregnancy category: C

(parenteral), Not rated (oral)

Indications

To treat chronic spastic conditions caused by severe chronic disorders, such as cerebral palsy, stroke, multiple sclerosis, and spinal cord injury Adults and adolescents. Initial: 25 mg daily for 7 days. Then dosage increased to 25 mg/ day every 4 to 7 days until desired response occurs or dosage reaches 100 mg q.i.d. Maximum: 400 mg daily. Children. Initial: 0.5 mg/kg b.i.d. for 7 days. Then increased by 0.5 mg/kg daily every 4 to 7 days until desired response occurs or dosage reaches 3 mg/kg q.i.d. Maximum: 400 mg daily. To prevent malignant hyperthermia before surgery Adults and children.4 to 8 mg/kg daily in divided doses t.i.d. or q.i.d. 1 or 2 days before surgery, with last dose given 3 to 4 hr before surgery.
IV: Adults and children. Initial: 2.5 mg/kg 60 to 75 min before anesthesia and infused over 1 hr. Additional individualized doses given as needed during surgery. To treat malignant hyperthermic crisis
I.V.INJECTION Adults and adolescents. Initial: 1 mg/kg by rapid bolus; repeated, p.r.n., until symptoms subside or cumulative dose of 10 mg/ kg has been reached and if symptoms reappear. To treat postmalignant hyperthermic crisis Adults and children.4 to 8 mg/kg daily in divided doses q.i.d. for 1 to 3 days.
I.V.INJECTION Adults and children. Initial: Individualized dosage beginning with 1 mg/kg or more as needed if oral therapy can’t be used. Maximum: 10 mg/kg total dose. Route Onset Peak Duration P.O. 1 wk* Unknown Unknown

Mechanism of Action

Acts directly on skeletal muscle to reduce the force of reflex muscle contraction. This in turn reduces hyperreflexia, spasticity, involuntary movements, and clonus, probably by preventing calcium release from the sarcoplasmic reticulum of skeletal muscle cells. Blocked calcium release also inhibits the activation of acute catabolism associated with malignant hyperthermic crisis syndrome.

Incompatibilities

Don’t administer parenteral dantrolene with acidic solutions, including D5W and normal saline solution.

Contraindications

For oral drug only: Active hepatic disease (such as cirrhosis and hepatitis), conditions in which spasticity helps maintain upright posture and improve balance or function, skeletal muscle spasms caused by rheumatic disorders

Interactions

calcium channel blockers (especially verapamil): Possibly hyperkalemia, shock, lifethreatening arrhythmias hepatotoxic : Increased risk of hepatotoxicity with long-term oral dantrolene use sedatives: Possibly profound sedation
alcohol use: Possibly increased CNS depression

Side Efect

CNS: Chills, confusion, depression, dizziness, drowsiness, fatigue, fever, headache, insomnia, light-headedness, malaise, nervousness, seizures, slurred speech or other speech problems, weakness
CV: Heart failure (I.V.), labile blood pressure, pericarditis, phlebitis, tachycardia
EENT: Abnormal vision, altered taste, diplopia, lacrimation
GI: Abdominal cramps, anorexia, constipation, diarrhea, dysphagia, gastric irritation, GI bleeding, hepatitis, hepatotoxicity
GU: Crystalluria, dysuria, erectile dysfunction, hematuria, nocturia, urinary frequency, urinary incontinence, urine retention
MS: Backache, myalgia
RESP: Feeling of suffocation, pleural effusion
SKIN: Acne, diaphoresis, eczematoid eruption, erythema (I.V.), extravasation with tissue damage, hirsutism, pruritus, rash, urticaria

Cautions

Use dantrolene cautiously in patients with impaired pulmonary function, especially dantrolene sodium 285 D * For spasticity; unknown for malignant hyperthermia. those with COPD, and in those with severe cardiac or hepatic dysfunction.

Reconstitute drug with 60 ml sterile water for injection.Shake vial until clear.Store reconstituted solution at room temperature,protected from direct sunlight.Discard after 6 hours.

To prevent precipitation, transfer reconstituted drug to a plastic I.V. bag, rather than a glass bottle, for infusion.

Because drug has a high pH, infuse into a central vein, if possible, to avoid tissue damage from extravasation.

Monitor blood pressure and heart rate often during administration to detect tachycardia and blood pressure changes.

Notify prescriber about persistent diarrhea with oral therapy; drug may need to be stopped.

Monitor results of liver function tests— especially ALT, AST, alkaline phosphatase, and total bilirubin levels—to detect hepatotoxicity. Expect to stop drug after 45 days if benefits aren’t sufficient because risk of hepatotoxicity increases with dose and time, especially for women and patients over age 35.

PATIENT SAFTY

Advise patient to take dantrolene with food if gastric irritation develops.

Tell patient that drug may weaken muscles used for walking and climbing stairs.

Explain drug’s sedating effects. Caution patient to avoid sedatives (unless prescribed), including alcohol.

Advise patient to report yellow skin or sclerae, itching, anorexia, and fatigue.

If patient misses a dose, tell her to wait until the next scheduled dose if more than 2 hours have passed since the missed dose. Instruct her not to double the dose.

Caution patient not to stop taking drug without consulting prescriber. Gradual dosage reduction may be required, especially after long-term use.

Category

Chemical class: Cyclic lipopeptide
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat complicated skin and skin structure infections caused by Staphylococcus aureus (including methicillinresistant isolates), Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus dysgalactiae subspecies Equisimilis, and Enterococcus faecalis (vancomycin-susceptible isolates only)
IV:
Adults.4 mg/kg administered over 30 min daily for 7 to 14 days. Maximum: 6 mg/kg I.V. every 24 hr.
DOSAGE ADJUSTMENT For patients with creatinine clearance less than 30 ml/min/ 1.73 m2, 4 or 6 mg/kg (depending on infection type) once every 48 hr. To treat Staphylococcus aureus bloodstream infections, including right-sided infective endocarditis, caused by methicillin-susceptible and methicillinresistant isolates
IV:
Adults. 6 mg/kg administered over 30 min daily for 2 to 6 wk. Maximum: 6 mg/kg I.V. every 24 hr.
DOSAGE ADJUSTMENT For patients with creatinine clearance less than 30 ml/min/ 1.73 m2, dosage is 4 or 6 mg/kg (depending on infection) once every 48 hr.

Mechanism of Action

Binds to bacterial membranes to cause rapid depolarization of membrane potential. This loss of membrane potential inhibits protein, DNA, and RNA synthesis, which results in bacterial cell death.

Contraindications

Hypersensitivity to daptomycin or its components

Interactions

HMG-CoA reductase inhibitors: Possibly increased CK level and increased risk of myopathy

Side Efect

CNS: Anxiety, asthenia, confusion, dizziness, fever, headache, insomnia, peripheral neuropathy
CV: Cardiac failure, chest pain, hypertension, hypotension, peripheral edema, supraventricular tachycardia
EENT: Pharyngolaryngeal pain, oral candaptomycin 286 didiasis, sore throat
ENDO: Hyperglycemia, hypoglycemia
GI: Abdominal pain, anorexia, constipation, diarrhea, dyspepsia, dysphagia, elevated liver enzymes, GI hemorrhage, nausea, pseudomembranous colitis, vomiting
GU: Renal failure, UTI, vaginal candidiasis
HEME: Anemia, eosinophilia, increased INR, leukocytosis, thrombocytopenia, thrombocytosis
MS: Arthralgia, back or limb pain, elevated myoglobin level, myopathy, rhabdomyolysis, osteomyelitis
RESP: Cough, dyspnea, pleural effusion, pneumonia, pulmonary eosinophilia, shortness of breath
SKIN: Cellulitis, diaphoresis, erythema, pruritus, rash, urticaria, vesiculobullous rash
Other: Anaphylaxis, bacteremia, elevated alkaline phosphatase level, elevated serum sodium bicarbonate level, fungal infection, hyperkalemia, hypokalemia, hypomagnesemia, injection site reactions, sepsis

Cautions

Obtain blood samples for culture and sensitivity testing before starting daptomycin.

Reconstitute daptomycin powder by slowly transferring 10 ml normal saline for injection into vial and pointing needle toward wall of vial to minimize foaming. Then gently rotate vial until all powder is wet. Don’t agitate or shake vial. Let vial stand undisturbed for 10 minutes, and then gently rotate or swirl contents for a few minutes, as needed, to obtain a completely reconstituted solution.

Further dilute reconstituted daptomycin solution with normal saline for injection, and give by I.V. infusion over 30 minutes. Reconstituted drug is stable in infusion bag for 12 hours at room temperature or 48 hours refrigerated.

Daptomycin may cause a significant false increase in PT and INR. If this occurs during daptomycin therapy, draw blood sample just before next daptomycin dose and evaluate other causes of the increase.

Monitor patient closely for diarrhea, which may herald pseudomebranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber. If pseudomembranous colitis develops, expect to discontinue drug and give fluids, electrolytes, protein, and antibiotic effective against C. difficile.

Monitor patient for evidence of superinfection, and inform prescriber if present. Expect to stop drug and provide care.

Assess patient for muscle pain or weakness, especially of distal limbs. Expect to monitor CK level weekly or more often in patients recently or currently taking an HMG-CoA reductase inhibitor. Expect to stop daptomycin, as ordered, if patient has myopathy or marked rise in CK level.

Monitor patient’s BUN and serum creatinine levels closely, especially if renal insufficiency is already present.

PATIENT SAFTY

Inform patient that diarrhea may occur 2 months or more after daptomycin therapy stops. If severe or prolonged, advise patient to notify prescriber as soon as possible; additional treatment may be needed.

Urge patient to immediately report muscle pain, tenderness, or weakness and other symptoms of myopathy.

Category

Chemical class: 165-amino acid glycoprotein identical to human erythropoietin
Therapeutic class: Antianemic

Pregnancy category: C

Indications

To treat anemia from chronic renal failure I.V.OR SUBCUTANEOUS INJECTION
Adults. Initial: 0.45 mcg/kg as a single dose every wk. Maintenance: Dosage individualized and increased monthly to maintain a hemoglobin level not to exceed 12 g/dl.
DOSAGE ADJUSTMENT Dosage reduced by about 25% if hemoglobin level increases and approaches 12 g/dl. If it continues to increase, doses temporarily withheld until hemoglobin level begins to decrease; then therapy is restarted at a dose about 25% below previous dose. Dosage reduced by about 25% if hemoglobin level increases by more than 1 g/dl in a 2-wk period. Dosage increased by about 25% of previous dose if hemoglobin level increases less than 1 g/dl darbepoetin alfa 287 D over 4 wk but only if serum ferritin level is 100 mcg/L or greater and serum transferrin saturation is 20% or greater. Further increases made at 4-wk intervals until specified hemoglobin level is obtained.
DOSAGE ADJUSTMENT For conversion from epoetin alfa to darbepoetin alfa, dosage administered every wk for patient who previously received epoetin alfa 2 to 3 times/ wk and once every 2 wk for patient who previously received epoetin alfa once/wk. For conversion from epoetin alfa, 6.25 mcg/ wk darbepoetin alfa given every wk for patients who received less than 2,500 units/ wk of epoetin alfa; 12.5 mcg/wk darbepoetin alfa every wk for patients who received 2,500 to 4,999 units/wk of epoetin alfa; 25 mcg/wk darbepoetin alfa every wk for patients who received 5,000 to 10,999 units/ wk of epoetin alfa; 40 mcg/wk darbepoetin alfa every wk for patients who received 11,000 to 17,999 units/wk of epoetin alfa; 60 mcg/wk darbepoetin alfa every wk for patients who received 18,000 to 33,999 units/ wk of epoetin alfa; 100 mcg/wk darbepoetin alfa every wk for patients who received 34,000 to 89,999 units/wk of epoetin alfa; 200 mcg/wk darbepoetin alfa every wk for patients who received 90,000 or more units/wk of epoetin alfa. To treat chemotherapy-induced anemia in patients with nonmyeloid malignancies and hemoglobin level less than 10 g/dl SUBCUTANEOUS INJECTION
Adults. Initial: 2.25 mcg/kg as a single dose every wk. Maintenance: Dosage individualized to maintain a target hemoglobin level.
DOSAGE ADJUSTMENT Dosage increased to 4.5 mcg/kg if hemoglobin level increases less than 1.0 g/dl after 6 wk of therapy. If it increases more than 1.0 g/dl over 2 wk or it exceeds 12 g/dl, dosage reduced by about 25%. If hemoglobin level exceeds 13 g/dl, doses temporarily withheld until it falls to 12 g/dl. Then therapy is restarted at a dose about 25% less than last dose given. Route Onset Peak Duration I.V., SubQ 2–6 wk Unknown Unknown

Mechanism of Action

Stimulates release of reticulocytes from the bone marrow into the bloodstream, where they develop into mature RBCs.

Incompatibilities

Don’t mix darbepoetin alfa with any other drug.

Contraindications

Hypersensitivity to human albumin or products made from mammal cells; uncontrolled hypertension

Side Efect

CNS: Asthenia, dizziness, fatigue, fever, headache, seizures, stroke, transient ischemic attack
CV: Acute MI, angina, arrhythmias, cardiac arrest, chest pain, congestive heart failure, hypertension, hypotension, peripheral edema, vascular access hemorrhage, vascular access thrombosis
GI: Abdominal pain, constipation, diarrhea, nausea, vomiting
MS: Arthralgia, back pain, limb pain, muscle spasm, myalgia
RESP: Bronchitis, cough, dyspnea, pneumonia, pulmonary embolism, upper respiratory tract infection
SKIN: Pruritus, rash, urticaria
Other: Dehydration, fluid overload, infection, flulike symptoms, injection site pain, sepsis

Cautions

Before starting darbepoetin alfa therapy, expect to correct folic acid or vitamin B12 deficiencies because these conditions may interfere with drug’s effectiveness.

Darbepoetin alfa shouldn’t be given to cancer patients when a cure is anticipated because drug may decrease survival rate and increase tumor progression in patients with certain types of cancers, such as breast, non-small cell lung, head and neck, lymphoid, and cervical cancers.

To ensure effective drug response, expect to obtain serum ferritin level and transferrin saturation before and during therapy, as ordered. If serum ferritin level is less than 100 mcg/L or serum transferrin saturation is less than 20%, expect to begin supplemental iron therapy.

Don’t shake vial during preparation to avoid denaturing drug and rendering it biologically inactive.

Discard drug if you see particulate matter or discoloration.

Don’t dilute drug before giving it. darbepoetin alfa 288

Needle cover on prefilled syringe contains dry natural rubber and may cause allergic reaction in those with latex sensitivity.

Discard unused portion of drug because it contains no preservatives.

Monitor patient closely for hypertension during therapy. Expect to reduce dosage or withhold drug if blood pressure is poorly controlled with antihypertensive and dietary measures.

Monitor hemoglobin level weekly, as ordered, until hemoglobin stabilizes and maintenance dosage has been achieved. Then monitor hemoglobin level regularly, as ordered. After each
DOSAGE ADJUSTMENT, expect to check hemoglobin level weekly for 4 weeks until it stabilizes in response to dosage change.
WARNING If hemoglobin level increases more than about 1 g/dl during any 2-week period or it exceeds 12 g/dl, the risk of cardiac arrest, seizures, stroke, worsened hypertension, congestive heart failure, vascular thrombosis, vascular ischemia, vascular infarction, acute MI, fluid overload with peripheral edema, tumor prgression, and shortened survival increases. Expect to decrease dosage if this occurs.

Expect to discontinue darbepoetin in cancer patients if hemoglobin level hasn’t increased after 8 weeks or if patient continues to need transfusions despite therapy.

Institute seizure precautions according to facility policy.

For patients with chronic renal failure who aren’t receiving dialysis, expect to give lower doses than those given to patients receiving dialysis. Also, monitor renal function test results and fluid and electrolyte balance in these patients for signs of declining renal function. If patient starts dialysis, monitor hemoglobin and blood pressure closely and expect maintenance dosage to be adjusted, as needed.

Store drug at 2° to 8° C (36° to 46° F). Don't freeze, and do protect from light.

PATIENT SAFTY

Advise patient that the risk of seizures is highest during the first 90 days of therapy. Discourage her from engaging in hazardous activities during this time.

Stress the importance of complying with the dosage regimen and keeping follow-up medical and laboratory appointments.

Advise patient to follow up with her prescriber for blood pressure monitoring.

Encourage patient to eat adequate quantities of iron-rich

If patient will self-administer darbepoetin, teach her and her caregiver the proper administration technique.

Caution patient and her caregiver not to reuse needles, syringes, or drug product. Thoroughly instruct them in proper needle and syringe disposal using a punctureresistant container.

Explain that needle cover on prefilled syringe contains dry natural rubber and may cause allergic reaction in those with latex sensivitity.

Review possible

Side Efect

, and urge patient to notify prescriber if she experiences chest pain, headache, rash, seizures, shortness of breath, or swelling.

Category

Chemical class: Muscarinic receptor antagonist
Therapeutic class: Bladder antispasmodic

Pregnancy category: C

Indications

To treat overactive urinary bladder with symptoms of urge incontinence, including urgency and frequency
Adults. Initial: 7.5 mg daily, increased to 15 mg daily after 2 wk as needed.
DOSAGE ADJUSTMENT For patients with moderate hepatic impairment and those taking potent CYP3A4 inhibitors (such as clarithromycin, itraconazole, ketoconazole, nefazodone, nelfinavir, and ritonavir) daily dosage should not exceed 7.5 mg. Route Onset Peak Duration P.O. Unknown 7 hr Unknown

Mechanism of Action

Antagonizes effect of acetylcholine on muscarinic receptors in detrusor muscle, decreasing muscle spasms that cause inappropriate bladder emptying. This action increases bladder capacity and volume, darifenacin 289 D which relieves sensations of urgency and frequency and enhances bladder control.

Contraindications

Gastric retention, hypersensitivity to darifenacin or its components, uncontrolled narrow-angle glaucoma, urine retention, and patients at risk for these conditions

Interactions

anticholinergics: Increased frequency and severity of anticholinergic

Side Efect

flecainide, thioridazine, tricyclic antidepressants: Risk of toxicity with these potent CYP3A4 inhibitors (such as clarithromycin, itraconazole, ketoconazole, nefazodone, nelfinavir, and ritonavir): Decreased metabolism and increased effects of darifenacin, possibly increasing the risk of

Side Efect

Side Efect

CNS: Asthenia, confusion, dizziness, hallucinations
CV: Hypertension, palpitations, peripheral edema
EENT: Abnormal vision, dry eyes or mouth, pharyngitis, rhinitis, sinusitis
GI: Abdominal pain, constipation, diarrhea, indigestion, nausea, vomiting
GU: Urine retention, UTI, vaginitis
MS: Arthralgia, back pain
RESP: Bronchitis
SKIN: Dry skin, pruritus, rash
Other: Angioedema, flulike symptoms, hypersensitivity reactions, weight gain

Cautions

Use darifenacin cautiously in patients with significant bladder outflow obstruction; they have increased risk of urine retention.

Use darifenacin cautiously in patients with severe constipation, ulcerative colitis, or myasthenia gravis because it may decrease GI motility. Also use drug cautiously in obstructive GI disorders because it increases the risk of gastric retention.

PATIENT SAFTY

Tell patient to swallow tablets with liquid and not to crush, split, or break them.

Advise patient to avoid exercising in hot weather because darifenacin decreases sweating, increasing the risk of heatstroke.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Category

Chemical class: Analogue of natural nucleoside 2'-deoxycytidine
Therapeutic class: Antineoplastic

Pregnancy category: D

Indications

To treat myelodysplastic syndromes (MDS) including secondary MDS of all French-American-British subtypes and intermediate 1 and 2 and high-risk International Prognostic Scoring System groups
IV:
Adults. 15 mg/m2over 3 hr, repeated every 8 hr for 3 days with cycle repeated every 6 wk for at least four cycles.
DOSAGE ADJUSTMENT For hematologic recovery that requires more than 6 wk but less than 8 wk, doses delayed for up to 2 wk and temporarily reduced to 11 mg/m2every 8 hr. For recovery that requires more than 8 wk but less than 10 wk, doses delayed up to 2 more wk and reduced to 11 mg/m2 every 8 hr, maintained or increased in subsequent cycles as clinically indicated.

Mechanism of Action

Inhibits DNA methyltransferase after phosphorylation and direct incorporation into DNA, resulting in hypomethylation of the DNA and cellular differentiation. In neoplastic cells, hypomethylation may restore normal function to genes essential for controlling cellular differentiation and proliferation. In rapidly dividing cells, decitabine also may cause cell death by forming covalent adducts between DNA methyltransferase and decitabine-saturated DNA.

Contraindications

Hypersensitivity to decitabine or its components

Side Efect

CNS: Anxiety, confusion, dizziness, fatigue, fever, headache, hypoesthesia, insomnia, lethargy, malaise, rigors
CV: Chest discomfort or pain, hypotension, peripheral edema
EENT: Bleeding gums, blurred vision, lip or decitabine 290 tongue ulceration, oral mucous petechiae, oral candidasis, pharyngitis, postnasal drip, sinusitis, stomatitis
ENDO: Hyperglycemia
GI: Abdominal distention, abdominal pain, anorexia, ascities, constipation, decreased appetite, diarrhea, dysphagia, dyspepsia, gastroesophageal reflux disease, hyperbilirubinemia, nausea, vomiting
GU: Dysuria, urinary frequency, UTI
HEME: Anemia, leukopenia, neutropenia, thrombocytopenia, thrombocythemia
MS: Arthralgia, back or limb pain, myalgia
RESP: Decreased breath sounds, cough, crackles, hypoxia, pneumonia, pulmonary edema
SKIN: Alopecia, cellulites, ecchymosis, erythema, hematoma, pallor, petechiae, pruritus, rash, urticaria
Other: Bacteremia; candidal infection; dehydration; facial edema; hyperkalemia; hypoalbuminemia; hypokalemia; hypomagnesemia; hyponatremia; injection site swelling, pain, and redness; lymphadenopathy

Cautions

Use cautiously in patients with liver or renal impairment.

Follow facility protocols for preparing and handling antineoplastic and for disposing of used equipment.

Reconstitute with 10 ml sterile water using aseptic technique; each milliliter contains about 5 mg of decitabine. Immediately after reconstitution, further dilute with normal saline solution, dextrose 5%, or lactated Ringer’s solution to a final concentration of 0.1 to 1 mg/ml. Use within 15 minutes. If delay is expected, reconstitute drug using cold dilution solution and store in refrigerator for up to 7 hours.

Monitor CBC—including hematocrit, platelet count, and WBC with differential—as well as electrolyte, liver enzyme, and serum creatinine levels before and intermittently during decitabine therapy, as ordered.

If patient develops leukopenia, look for evidence of infection, such as fever. Expect to obtain appropriate specimens for culture and sensitivity testing.
WARNING Monitor patient closely for nonhematologic toxicities, such as active or uncontrolled infection, serum creatinine level greater than 2 mg/dl, or serum glutamic pyruvic transaminase or total bilirubin 2 or more times the upper limit of normal. If present, notify prescriber and expect decitabine therapy to be withheld until resolved.

PATIENT SAFTY

Advise male patients not to father a child during decitabine therapy and for 2 months after. Also urge female patients to use contraception to avoid pregnancy during therapy and to notify prescriber immediately if pregnancy occurs.

Urge patient to have needed dental work completed before starting decitabine therapy, if possible, or to defer such work until blood counts return to normal because decitabine can delay healing and cause gingival bleeding. Teach patient proper oral hygiene, and advise him to use a softbristled toothbrush.

If patient develops bone marrow depression, instruct him to avoid people with infections and to report fever, cough, or lower back or side pain; they may indicate infection.

Stress the need to avoid accidental cuts from sharp objects, such as razor blades or fingernail clippers, because excessive bleeding or infection may occur.

Advise patient with stomatitis to eat bland, soft served cold or at room temperature to decrease irritation.

Stress the need to comply with the dosage regimen and to keep follow-up medical and laboratory appointments.

Category

Chemical class: Benzoic acid
Therapeutic class: Iron chelator

Pregnancy category: B

Indications

To treat chronic iron overload caused by blood transfusions Adults and children age 2 and over.Initial: 20 mg/kg/day, increased by 5 to 10 mg/kg every 3 to 6 mo. Maximum: 30 mg/kg/day. deferasirox 291 D

Mechanism of Action

Binds iron with high affinity and removes it in feces. Deferasirox is a tridentate ligan. Route Onset Peak Duration P.O. Unknown 1.5–4 hr Unknown

Contraindications

Hypersensitivity to deferasirox or its components, hearing impairment

Interactions

aluminum-containing antacids, phenobarbital, phenytoin, rifampicin, ritonavir: Possibly decreased effectiveness of deferasirox anticoagulants, corticosteroids, NSAIDs, oral bisphosphonates: Increased risk of GI ulceration or hemorrhage cyclosporine, hormonal contraceptives, midazolam, simvastatin: Possibly decreased effectiveness of these iron chelators: Possibly combined effect paclitaxel, repaglinide: Increased plasma levels and effects of these food: Increased bioavailability of deferasirox

Side Efect

CNS: Dizziness, fatigue, fever, headache, hyperactivity, insomnia
EENT: Acute tonsillitis, cataracts, decreased hearing, ear infection, elevated intraocular pressure, high-frequency hearing loss, lens opacities, nasopharyngitis, pharyngolaryngeal pain, pharyngitis, retinal disturbances, rhinitis
GI: Abdominal pain, diarrhea, elevated liver enzymes, gallstones, hepatic failure, hepatitis, nausea, pancreatitis, upper GI ulceration and hemorrhage, vomiting
GU: Acute renal failure, glycosuria, increased creatinine, proteinuria, renal tubulopathy
HEME: Agranulocytosis, neutropenia, thrombocytopenia
MS: Arthralgia, back pain
RESP: Bronchitis, cough, respiratory tract infection
SKIN: Leukocytoclastic vascultitis, purpura, rash, urticaria
Other: Anaphylaxis, angioedema, drug fever, influenza

Cautions

Because deferasirox can cause renal failure, obtain baseline assessment of patient’s renal function by collecting blood samples to measure serum creatinine level twice before starting deferasirox. When therapy starts, monitor serum creatinine level, as ordered, especially in elderly patients, patients taking other that depress renal function, and patients with increased risk of complications, pre-existing renal conditions, or comorbid conditions. For patients at increased risk for renal failure, expect to monitor serum creatinine level weekly for first month of therapy and monthly thereafter. Report increased serum creatinine level, and expect deferasirox dosage to be decreased.

Because deferasirox may cause hepatic abnormalities and failure, obtain baseline assessment of hepatic function before therapy starts by collecting blood samples to measure liver enzymes and bilirubin level. When therapy starts, monitor these levels every 2 weeks for first month and then monthly thereafter. Notify prescriber about elevations, and expect to decrease dose for severe or persistent elevations.

Obtain auditory and ophthalmic testing (including slit lamp examination and dilated fundoscopy) before deferasirox therapy begins and yearly thereafter, as ordered, because drug infrequently causes auditory or visual disturbances.

Monitor patient’s blood counts regularly, as ordered, because deferasirox can cause cytopenias. If cytopenia occurs, expect drug to be discontinued until blood counts return to normal.

Especially in the first month of therapy, assess patient closely for hypersensitivity reactions, such as anaphylaxis or angioedema. Notify prescriber immediately if present, and expect drug to be discontinued. Provide care, as needed.

Inspect patient’s skin regularly for rash. If it occurs and becomes severe, drug may be withheld temporarily.

Watch for evidence of GI ulceration and hemorrhage, especially if patient takes that increase the risk of ulceration and bleeding, such as NSAIDs, corticosteroids, oral bisphosphonates, or anticoagulants. Notify prescriber of suspected GI ulceration or hemorrhage, and prepare patient for further evaluation and treatdeferasirox 292 ment, as prescribed.

PATIENT SAFTY

Instruct patient to take deferasirox 30 minutes before eating. Tell her to completely disperse the tablet in water, orange juice, or apple juice; drink the suspension immediately; and then add liquid to any remaining residue and drink again.

Tell patient to avoid taking aluminumbased antacids at the same time as deferasirox and to seek prescriber advice before taking other , including OTC preparations such as NSAIDs, because of potential interactions.

Advise her to report any hearing or visual disturbances.

If patient has diarrhea or vomiting, tell her to notify prescriber and to stay hydrated.

Caution her to avoid hazardous activities, such as driving, if she becomes dizzy.

Category

Chemical class: Tetracycline derivative
Therapeutic class: Antibiotic

Pregnancy category: D

Indications

To treat Rocky Mountain spotted fever, typhus infections, Q fever, and rickettsialpox and tick fevers caused by Rickettsieae; psittacosis (ornithosis), lymphogranuloma venereum, granuloma inguinale, and Mycoplasma pneumoniae or Borrelia recurrentis infections; infections caused by gramnegative organisms, such as Bacteroides species, Bartonella bacilliformis, Brucella species, Campylobacter fetus, Francisella tularensis, Haemophilus ducreyi,Vibrio cholerae, and Yersinia pestis; infections caused by susceptible strains of Acinetobacter calcoaceticus, Enterobacter aerogenes, Escherichia coli, Haemophilus influenzae (respiratory tract infections), Herellea species, Klebsiella species (respiratory tract infections and UTIs), and Shigella species; infections caused by susceptible strains of Staphylococcus aureus (skin and soft-tissue infections) and Streptococcus species; infections caused by Actinomyces species, Bacillus anthracis, Clostridium species, Fusobacterium fusiforme, Listeria monocytogenes, Treponema pallidum, and Treponema pertenue; and acute intestinal amebiasis , Adults and adolescents. 150 mg every 6 hr or 300 mg every 12 hr. Children ages 8 to 12. 6 to 12 mg/kg daily in divided doses every 6 to 12 hr. To treat gonorrhea , Adults and adolescents.600 mg followed by 300 mg every 12 hr for 4 days for total dose of 3,000 mg.

Mechanism of Action

Binds with ribosomal subunits of susceptible bacteria and alters the cytoplasmic membrane, inhibiting bacterial protein synthesis and rendering organism ineffective.

Contraindications

Hypersensitivity to demeclocycline or other tetracyclines

Interactions

antacids, calcium supplements, cholestyramine, choline, colestipol, iron supplements, magnesium-containing laxatives, magnesium salicylate, sodium bicarbonate: Decreased demeclocycline absorption digoxin: Possibly increased blood digoxin level and risk of digitalis toxicity
methoxyflurane: Increased nephrotoxicity oral anticoagulants: Increased anticoagulation oral contraceptives: Decreased contraceptive effectiveness penicillins: Decreased bactericidal action of penicillins vitamin A: Possibly benign intracranial hypertension milk, other dairy products: Decreased drug absorption

Side Efect

CNS: Dizziness, headache, light-headedness, vertigo
EENT: Tinnitus, vision changes
GI: Abdominal cramps, diarrhea, nausea, demeclocycline hydrochloride 293 D pseudomembranous colitis, vomiting
GU: Elevated BUN level, nephrogenic diabetes insipidus
HEME: Eosinophilia, hemolytic anemia, neutropenia, thrombocytopenia
SKIN: Photosensitivity, pruritus, rash, urticaria
Other: Anaphylaxis, angioedema

Cautions

Expect to monitor renal and liver function tests during demeclocycline therapy.
WARNING Watch for nephrogenic diabetes insipidus during long-term therapy.

Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold demeclocycline and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

PATIENT SAFTY

Stress importance of completing therapy as prescribed, even if symptoms improve.

Advise patient not to take demeclocycline within 3 hours of other or dairy products; its absorption may decrease.

Instruct patient to avoid taking antacids because of impaired drug absorption.

Advise patient to avoid direct sunlight, use sunscreen, and wear protective clothing outdoors; among tetracyclines, demeclocycline causes the most photosensitivity.

Urge patient to immediately report edema, rash, or other hypersensitivity reactions.

Urge patient to report watery, bloody stools to prescriber immediately, even up to 2 months after drug therapy has ended.

Tell patient to avoid hazardous activities if light-headed, dizzy, or vertigo occurs.

Instruct woman of childbearing age to notify prescriber if she may be pregnant; drug may need to be discontinued.

Category

Chemical class: Dibenzazepine derivative
Therapeutic class: Antidepressant

Pregnancy category: C

Indications

To treat depression
Adults.Initial: 100 to 200 mg daily as single dose or divided doses. Increased gradually to 300 mg daily, if needed. Maximum: 300 mg daily. Adolescents.Initial: 25 to 50 mg daily in divided doses. Increased gradually, if needed. Maximum: 100 mg daily. Children ages 6 to 12. Initial: 10 to 30 mg daily, or 1 to 5 mg/kg, in divided doses.
DOSAGE ADJUSTMENT For elderly patients, initial dosage decreased to 25 to 50 mg daily in divided doses; increased gradually, if needed,, to maximum of 150 mg daily. Route Onset Peak Duration P.O. 2–3 wk Unknown Unknown

Mechanism of Action

Blocks serotonin and norepinephrine reuptake by adrenergic nerves, which normally release these neurotransmitters from their storage sites when activated by a nerve impulse. By blocking reuptake, this tricyclic antidepressant increases serotonin and norepinephrine levels at nerve synapses, which may elevate mood and reduce depression.

Contraindications

Acute recovery phase of MI; hypersensitivity to desipramine, other tricyclic antidepressants, or their components; MAO inhibitor therapy within 14 days

Interactions

activated charcoal: Prevention of desipramine absorption, reduced effects barbiturates: Decreased blood desipramine level, increased CNS depression bupropion, haloperidol, H2-receptor antagonists,
valproic acid: Increased blood level and adverse effects of desipramine carbamazepine: Increased blood carbamazepine level, decreased blood desipramine level
cimetidine: Increased blood desipramine level and anticholinergic effects (dry mouth, urine retention, blurred vision)
clonidine: Increased risk of hypertensive crisis dicumarol: Increased anticoagulant effect grepafloxacin, quinolones, sparfloxacin: Increased risk of arrhythmias, including desipramine hydrochloride 294 torsades de pointes guanethidine: Antagonized antihypertensive effect of guanethidine levodopa: Delayed levodopa absorption, increased risk of hypotension
MAO inhibitors: Increased risk of lifethreatening adverse effects, such as hyperpyretic or hypertensive crisis and severe seizures phenothiazines: Increased desipramine level, risk of inhibited phenothiazine metabolism and neuroleptic malignant syndrome
quinidine: Increased blood quinidine level rifamycins: Decreased desipramine effects selective serotonin reuptake inhibitors: Increased desipramine effects sympathomimetics: Possibly arrhythmias, possibly increased or decreased vasopressor effects of sympathomimetics
alcohol use: Possibly increased CNS or respiratory depression, hypotension, alcohol effects

Side Efect

CNS: Agitation, akathisia, anxiety, ataxia, confusion, delusions, disorientation, dizziness, drowsiness, extrapyramidal reactions, fatigue, headache, hypomania, insomnia, lack of coordination, nervousness, nightmares, paresthesia, peripheral neuropathy, psychosis exacerbation, restlessness, seizures, sleep disturbance, stroke, suicidal ideation (children and teens), tremor, weakness
CV: Arrhythmias, including heart block; hypertension; hypotension; palpitations
EENT: Black tongue, blurred vision, dry mouth, mydriasis, stomatitis, taste perversion, tinnitus
ENDO: Breast enlargement and galactorrhea (women), gynecomastia (men), hyperglycemia, hypoglycemia, syndrome of inappropriate ADH secretion
GI: Abdominal cramps, anorexia, constipation, diarrhea, elevated liver function test results, elevated pancreatic enzyme levels, epigastric distress, hepatitis, ileus, increased appetite, nausea, vomiting
GU: Acute renal failure, impotence, libido changes, nocturia, painful ejaculation, testicular swelling, urinary frequency and hesitancy, urine retention
HEME: Agranulocytosis, eosinophilia, thrombocytopenia
SKIN: Acne, alopecia, dermatitis, diaphoresis, dry skin, flushing, petechiae, photosensitivity, pruritus, purpura, rash, urticaria
Other: Angioedema, drug fever, weight gain

Cautions

Use desipramine with extreme caution in patients with cardiovascular disease, glaucoma, seizure disorder, thyroid disease, or urine retention or with a family history of sudden death, cardiac arrhythmias, or conduction disturbances.
WARNING Desipramine increases risk of suicidal ideation in children and teens; monitor them closely for evidence.
WARNING Expect drug to produce sedation and possibly to lower seizure threshold. Take safety and seizure precautions. Seizures may precede arrhythmias and death in some patients. Alert prescriber immediately if seizure activity occurs.

Monitor blood glucose level often.

Be prepared to obtain blood sample for leukocyte and differential counts if patient develops fever during therapy.

Expect to discontinue drug as soon as possible before elective surgery because of its possible adverse cardiovascular effects.

PATIENT SAFTY

WARNING Urge parents to watch child or teen closely and to report abnormal thinking or behavior, aggression, or hostility.

Urge patient to use sunscreen outdoors and to avoid sunlamps and tanning beds.

Instruct patient to notify prescriber immediately about a fast and pounding heartbeat, fainting, severe agitation or restlessness, and strange behavior or thoughts.

Caution patient not to stop drug abruptly; doing so may cause dizziness, headache, hyperthermia, irritability, malaise, nausea, sleep disturbances, and vomiting.

Advise against drinking alcohol because of increased risk of adverse CNS reactions.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Urge diabetic patient to monitor blood glucose level often.

Category

Chemical class: Synthetic ADH analogue
Therapeutic class: Antidiuretic, antihemorrhagic

Pregnancy category: B

Indications

To manage primary nocturnal enuresis Adults and children age 6 and over. Initial: 0.2 mg at bedtime, increased as needed. Maximum: 0.6 mg daily. To control symptoms of central diabetes insipidus Adults and children age 6 and over. Initial: 0.05 mg b.i.d., increased as needed. Usual: 0.1 to 0.8 mg in divided doses b.i.d. or t.i.d. Maximum: 1.2 mg daily.
IV:, I.M.OR SUBCUTANEOUS INJECTION
Adults. 2 to 4 mcg daily in divided doses b.i.d. Dosage adjusted as needed. NASAL SOLUTION Adults and adolescents. 0.1 to 0.4 ml daily (10 to 40 mcg daily) as a single dose or in divided doses b.i.d. or t.i.d. Dosage adjusted as needed. If daily dose is divided, each dose adjusted separately. Children ages 3 months to 12 years. 0.25 mcg/kg daily as a single dose or in divided doses b.i.d. Dosage adjusted as needed. If daily dose is divided, each dose adjusted separately. To prevent or manage bleeding episodes in hemophilia A or mild to moderate type I von Willebrand’s disease
IV: Adults and children weighing more than 10 kg (22 lb). 0.3 mcg/kg diluted in 50 ml of normal saline solution and infused over 15 to 30 min. If used preoperatively, given 30 min before procedure. Children weighing 10 kg or less. 0.3 mcg /kg diluted in 10 ml normal saline solution and infused over 15 to 30 min. If used preoperatively, given 30 min before procedure. NASAL SOLUTION(STIMATE
NASAL SPRAY) Adults and children weighing more than 50 kg (110 lb). 150 mcg in each nostril. If used preoperatively, given 2 hr before procedure. Adults and children weighing 50 kg or less.150 mcg in one nostril. If used preoperatively, given 2 hr before procedure. Route Onset Peak Duration P.O. 1 hr* 4–7 hr* 8–12 hr* I.V. 15–30 min30–60 min3 hr Nasal In 1 hr* 1–5 hr* 8–20 hr*

Mechanism of Action

Exerts an antidiuretic effect similar to that of vasopressin by increasing cellular permeability of renal collecting ducts and distal tubules, thus enhancing water reabsorption, reducing urine flow, and increasing osmolality. As an antihemorrhagic, drug increases blood level of clotting factor VIII (antihemophilic factor) and activity of von Willebrand factor (factor VIIVWF). It also may increase platelet aggregation and adhesion at injury sites by directly affecting blood vessel walls.

Contraindications

Hypersensitivity to desmopressin or its components, moderate to severe renal impairment (creatinine clearance below 50 ml/min/1.73 m2), previous or current hyponatremia

Interactions

carbamazepine, chlorpromazine, lamotrigine, NSAIDs, opioid analgesics, selective serotonin reuptake inhibitors, tricyclic antidepressants: Possibly increased risk of water intoxication with hyponatremia demeclocycline, lithium: Possibly decreased antidiuretic effect of desmopressin imipramine, oxybutinin: Increased risk of hyponatremic seizures vasopressor : Possibly potentiated vasopressor effect of desmopressin

Side Efect

CNS: Asthenia, chills, dizziness, headache, stroke
CV: Hypertension (with high doses), MI, desmopressin acetate 296 * For antidiuretic effect. For antihemorrhagic effect. For von Willebrand disease; 4 to 20 hr for mild hemophilia A. thrombosis, transient hypotension
EENT: Conjunctivitis, epistaxis, lacrimation, nasal congestion (nasal form), ocular edema, pharyngitis, rhinitis
GI: Nausea
GU: Vulvar pain (parenteral form)
SKIN: Flushing
Other: Anaphylaxis, hyponatremia, injection site pain and redness; water intoxication

Cautions

Use desmopressin cautiously in patients with conditions associated with fluid and electrolyte imbalance, such as cystic fibrosis, heart failure, and renal disorders; these patients are prone to hyponatremia.

Also use cautiously in patients with habitual or psychogenic polydipsia; they may be more likely to drink excessive water, raising the risk of hyponatremia.

Nasal cavity scarring, edema, and other abnormalities may cause erratic absorption and require a different administration route.

Check blood pressure often during therapy.
WARNING Monitor patient closely for evidence of hyponatremia, such as headache, nausea, vomiting, restlessness, fatigue, lethargy, depressed reflexes, and changes in mental status. If left undetected, seizures, coma, and respiratory arrest may occur. Monitor patient’s serum sodium level, and notify prescriber of abnormalities.

PATIENT SAFTY

To prevent hyponatremia and water intoxication in a child or an elderly patient, urge family to restrict patient’s fluids as prescribed.

Tell patient to refrigerate nasal solution.

Teach patient to prime
NASAL SPRAY pump (only once) and spray dose into one or both nostrils, as prescribed, while inhaling briskly. Instruct her to clean tip of sprayer with hot water and dry it with clean tissue. Advise her to keep track of doses given and to discard bottle after 50 doses.

Instruct patient who uses Stimate Nasal Spray to prime pump before first use by pressing down four times. Advise her to discard pump after 25 or 50 doses, depending on bottle, because delivery of an accurate dose can’t be assured.

For nasal tube, teach patient to draw prescribed amount of solution into calibrated plastic tube, insert one end of tube into a nostril and the other end into her mouth, and gently blow into tube to deposit solution deep into nasal cavity. Caution her not to let drug drain into her mouth.

Teach patient or caregiver how to administer subcutaneous injection, if appropriate.

Urge patient to report side efect

Category

Chemical class: Synthetic adrenocortical steroid
Therapeutic class: Anti-inflammatory, diagnostic aid, immunosuppressant

Pregnancy category: C

Indications

To treat endocrine disorders, such as congenital adrenal hyperplasia, hypercalcemia associated with cancer, and nonsuppurative thyroiditis; acute episodes or exacerbations of rheumatic disorders; collagen diseases, such as systemic lupus erythematosus and acute rheumatic carditis; severe dermatologic diseases; severe allergic conditions, such as seasonal or perennial allergic rhinitis, bronchial asthma, serum sickness, and drug hypersensitivity reactions; respiratory diseases, such as symptomatic sardexamethasone 297 D coidosis, Löffler’s syndrome, berylliosis, fulminating or disseminated pulmonary tuberculosis, and aspiration pneumonitis; hematologic disorders, such as idiopathic thrombocytopenic purpura and secondary thrombocytopenia in adults, autoimmune hemolytic anemia, aplastic crisis, and congenital hypoplastic anemia; tuberculous meningitis and trichinosis with neurologic or myocardial involvement To manage leukemias and lymphomas in adults and acute leukemia in children; to induce diuresis or remission of proteinuria in idiopathic nephrotic syndrome without uremia or nephrotic syndrome caused by systemic lupus erythematosus To provide palliative therapy during acute exacerbations of GI diseases, such as ulcerative colitis and regional enteritis ELIXIR,,, I.V.OR I.M. INJECTION
Adults.Highly individualized dosage based on severity of disorder. Usual: 0.75 to 9 mg/ day as a single dose or in divided doses. ELIXIR,, Children. Highly individualized based on severity of disorder.Usual: 83.3 to 333.3 mcg/ kg daily in divided doses t.i.d. or q.i.d.
I.M.INJECTION Children. Highly individualized based on severity of disorder. Usual: 27.76 to 166.65 mcg/kg every 12 to 24 hr. To manage adrenocortical insufficiency ELIXIR,,, I.V.OR I.M. INJECTION
Adults. 0.5 to 9 mg daily as a single dose or in divided doses. ELIXIR,, Children.23.3 mcg/kg daily in divided doses t.i.d.
I.M.INJECTION Children. 23.3 mcg/kg daily in divided doses t.i.d. given every third day; alternatively, 7.76 to 11.65 mcg/kg daily. To test for Cushing’s syndrome ELIXIR,,
Adults. 0.5 mg every 6 hr for 48 hr followed by collection of 24-hr urine specimen to determine 17-hydroxycorticosteroid level. Or, 1 mg at 11 p.m. followed by plasma cortisol test performed at 8 a.m. the next day. To distinguish Cushing’s syndrome related to pituitary corticotropin excess from Cushing’s syndrome from other causes ELIXIR,,
Adults.2 mg every 6 hr for 48 hr followed by collection of 24-hr urine specimen to determine 17-hydroxycorticosteroid level. To decrease cerebral edema ELIXIR,,
Adults. 2 mg every 8 to 12 hr as maintenance after parenteral form has controlled initial symptoms. I.V.OR
I.M.INJECTION
Adults. 10 mg I.V. followed by 4 mg I.M. every 6 hr. Decreased after 2 to 4 days, if needed, gradually tapering off over 5 to 7 days unless inoperable or recurring brain tumor is present. If such a tumor is present, dosage gradually decreased after 2 to 4 days to maintenance dosage of 2 mg I.M. every 8 to 12 hr and switched to P.O. regimen as soon as possible. To treat unresponsive shock
IV: AND INJECTION
Adults.20 mg as a single dose followed by 3 mg/kg over 24 hr as a continuous infusion; 40 mg as a single dose followed by 40 mg every 2 to 6 hr, as needed; or 1 mg/kg as a single dose. All regimens used no more than 3 days. To decrease localized inflammation INTRA-ARTICULAR INJECTION
Adults.2 to 4 mg for large joint; 0.8 to 1 mg for small joint; 2 to 3 mg for bursae; 0.4 to 1 mg for tendon sheaths. SOFT-TISSUE INJECTION
Adults.2 to 6 mg; 1 to 2 mg for ganglia. INTRALESIONAL INJECTION
Adults.0.8 to 1.6 mg/injection site. To decrease inflammation in allergic conditions or nasal polyps (except in sinuses) NASAL AEROSOL Adults and children age 12 and over. 2 sprays (0.2 mg) in each nostril b.i.d. or t.i.d. Maximum: 12 sprays (1.2 mg) daily. Children ages 6 to 12. 1 or 2 sprays (0.1 to 0.2 mg) in each nostril b.i.d. Maximum: 8 sprays (0.8 mg) daily.

Mechanism of Action

Binds to intracellular glucocorticoid receptors and suppresses inflammatory and immune responses by:

inhibiting neutrophil and monocyte accudexamethasone 298 mulation at inflammation site and suppressing phagocytic and bactericidal action

stabilizing lysosomal membranes

suppressing antigen response of macrophages and helper T cells

inhibiting synthesis of inflammatory response mediators, such as cytokines, interleukins, and prostaglandins.

Contraindications

Administration of live-virus vaccine to patient or family member, hypersensitivity to dexamethasone or its components (including sulfites), idiopathic thrombocytopenic purpura (I.M. administration), systemic fungal infections

Interactions

aminoglutethimide, antacids, barbiturates, carbamazepine, hydantoins, mitotane,
rifampin: Decreased dexamethasone effects amphotericin B (parenteral), carbonic anhydrase inhibitors: Risk of hypokalemia anticholinesterases: Decreased anticholinesterase effectiveness in myasthenia gravis aspirin,
NSAIDs: Increased risk of adverse GI effects cholestyramine: Increased dexamethasone clearance cyclosporine: Increased activity of both , possibly resulting in seizures digoxin: Increased risk of digitalis toxicity related to hypokalemia ephedrine: Decreased half-life and increased clearance of dexamethasone erythromycin, indinavir: Increased clearance and decreased levels of these estrogens, ketoconazole, macrolide antibiotics: Decreased dexamethasone clearance isoniazid: Decreased blood isoniazid level neuromuscular blockers: Possibly potentiated or counteracted neuromuscular blockade oral anticoagulants: Altered coagulation times, requiring reduced anticoagulant dosage oral contraceptives: Increased half-life and concentration of dexamethasone
phenytoin: Increased risk of seizures potassium-wasting diuretics: Increased potassium loss and risk of hypokalemia salicylates: Decreased blood level and effectiveness of salicylates somatrem: Possibly inhibition of somatrem’s growth-promoting effect thalidomide: Increased risk of toxic epidermal necrolysis theophyllines: Altered effects of either drug toxoids, vaccines: Decreased antibody response
alcohol use: Increased risk of GI bleeding

Side Efect

CNS: Depression, emotional lability, euphoria, fever, headache, increased ICP with papilledema, insomnia, light-headedness, malaise, neuritis, neuropathy, paresthesia, psychosis, seizures, syncope, tiredness, vertigo, weakness
CV: Arrhythmias, bradycardia, edema, fat embolism, heart failure, hypercholesterolemia, hyperlipidemia, hypertension, myocardial rupture, tachycardia, thromboembolism, thrombophlebitis, vasculitis
EENT: Cataracts, glaucoma, vision changes (all forms); epistaxis, loss of smell and taste, nasal burning and dryness, oral candidiasis, perforated nasal septum, pharyngitis, rebound nasal congestion, rhinorrhea, sneezing (nasal aerosol)
ENDO: Cushingoid symptoms, decreased iodine uptake, growth suppression in children, hyperglycemia, menstrual irregularities, secondary adrenocortical and pituitary unresponsiveness
GI: Abdominal distention, bloody stools, elevated liver function test results, heartburn, hepatomegaly, increased appetite, indigestion, intestinal perforation, melena, nausea, pancreatitis, peptic ulcer with possible perforation, ulcerative esophagitis, vomiting
GU: Glycosuria, increased or decreased number and motility of spermatozoa, perineal irritation, urinary frequency
HEME: Leukocytosis, leukopenia
MS: Aseptic necrosis of femoral and humeral heads; muscle atrophy, spasms, or weakness; myalgia; osteoporosis; pathologic fracture of long bones; tendon rupture (intra-articular injection); vertebral compression fracture
RESP: Bronchospasm
SKIN: Acne, allergic dermatitis, diaphoresis, ecchymosis, erythema, hirsutism, necrotizing vasculitis, petechiae, subcutaneous fat atrophy, striae, thin and fragile skin, urticaria
Other: Aggravated or masked signs of infection, anaphylaxis, angioedema, hypernatremia, hypocalcemia, hypokalemia, dexamethasone 299 D hypokalemic alkalosis, impaired wound healing, metabolic acidosis, sodium and fluid retention, suppressed skin test reaction, weight gain

Cautions

Use dexamethasone cautiously in patients with congestive heart failure, hypertension, or renal insufficiency because drug can cause sodium retention, which may lead to edema and hypokalemia.

Also use cautiously in patients who have had intestinal sugery and in those with peptic ulcer, diverticulitis, or ulcerative colitis because of the risk of perforation.

Give once-daily dose of dexamethasone in the morning to coincide with the body’s natural cortisol secretion.

Give oral drug with food to decrease GI distress.

Be aware that dosage forms with a concentration of 24 mg/ml are for I.V. use only.

Shake I.M. solution before injecting deep into large muscle mass.
WARNING Avoid subcutaneous injection; it may cause atrophy and sterile abscess.

Inject undiluted I.V. dose directly into I.V. tubing of infusing compatible solution over 30 seconds or less, as prescribed.
WARNING Don’t give acetate form by I.V. injection.

Shake nasal aerosol container well, and hold it upright about 60 (15 cm) from area being treated. Keep spray out of patient’s eyes, and advise her not to inhale it.

Expect to taper drug rather than stopping it abruptly; prolonged use can cause adrenal suppression.

Monitor fluid intake and output and daily weight, and watch for crackles, dyspnea, peripheral edema, and steady weight gain.

Evaluate growth if patient is a child.

Test stool for occult blood.

Monitor results of hematology studies and blood glucose, serum electrolyte, cholesterol, and lipid levels. Dexamethasone may cause hyperglycemia, hypernatremia, hypocalcemia, hypokalemia, or leukopenia. It also may increase serum cholesterol and lipid levels, and it may decrease iodine uptake by the thyroid.

Assess patient for evidence of osteoporosis, Cushing’s syndrome, and other systemic effects during long-term use.

Monitor neonate for signs of hypoadrenocorticism if mother received dexamethasone during pregnancy. Be aware that some preparations contain benzyl alcohol, which may cause a fatal toxic syndrome in neonates and immature infants.

Watch for hypersensitivity reactions after giving acetate or sodium phosphate form; both may contain bisulfites or parabens, to which some people are allergic.

PATIENT SAFTY

Instruct patient not to store drug in damp or hot places and to protect liquid form from freezing.

Instruct patient to take once-daily oral dose in the morning with food to help prevent GI distress.

Caution against consuming alcohol during dexamethasone therapy because it increases the risk of GI bleeding.

Advise patient to follow a low-sodium, high-potassium, high-protein diet, if prescribed, to help minimize weight gain, which is common with dexamethasone therapy. Instruct her to inform prescriber if she’s on a special diet.

Instruct patient not to stop drug abruptly.

Advise patient to notify prescriber if condition recurs or worsens after dosage is reduced or therapy stops.

Urge patient to have regular eye examinations during long-term use.

Advise patient on long-term therapy to carry medical identification and to notify all health care providers that she takes dexamethasone.

Instruct patient (especially a child) to avoid close contact with anyone who has chickenpox or measles and to notify prescriber immediately if exposure occurs.

Advise patient and family members to avoid live-virus vaccinations during therapy unless prescriber approves.

Inform diabetic patient that drug may affect her blood glucose level.

If drug is injected into a joint, instruct patient to avoid putting excessive pressure on it and to notify prescriber if it becomes red or swollen.

Tell patient to notify prescriber about anorexia, depression, light-headedness, malaise, muscle pain, nausea, vomiting, and early hyperadrenocorticism (abdominal distention, amenorrhea, easy bruising, extreme weakness, facial hair, increased dexamethasone 300 appetite, moon face, weight gain). Tell patient and family about possible changes in appearance.

Urge patient to notify prescriber about illness, surgery, or changes in stress level.

Category

Chemical class: Propylamine derivative
Therapeutic class: Antihistamine

Pregnancy category: B

Indications

To treat allergic conjunctivitis; transfusion reaction; dermographism; mild, uncomplicated allergic skin reactions, such as urticaria and angioedema; perennial and seasonal allergic rhinitis; and vasomotor rhinitis and as adjunct to treat anaphylaxis Adults and adolescents.4 to 6 mg daily at bedtime or every 8 to 10 hr, p.r.n. SYRUP, Adults and adolescents. 2 mg every 4 to 6 hr, p.r.n. Children ages 6 to 12. 1 mg every 4 to 6 hr or 150 mcg/kg in divided doses q.i.d., p.r.n. Children ages 2 to 6. 0.5 mg every 4 to 6 hr, p.r.n. Route Onset Peak Duration P.O. 15–60 Unknown* 4–8 hr* min*

Mechanism of Action

Binds to central and peripheral H1receptors, competing with histamine for these sites and preventing histamine from reaching its site of action. By blocking histamine, dexchlorpheniramine:

inhibits respiratory, vascular, and GI smooth-muscle contraction, which prevents wheezing

decreases capillary permeability, which reduces itching, flares, and wheals

decreases lacrimal and salivary gland secretions, reducing nasal secretions, itching, sneezing, and watery eyes.

Contraindications

Angle-closure glaucoma; benign prostatic hyperplasia; bladder neck obstruction; hypersensitivity to dexchlorpheniramine or other antihistamines; lower respiratory tract disorders, such as asthma; MAO inhibitor use within 14 days; pyloroduodenal obstruction; stenosing peptic ulcer

Interactions

anticholinergics: Potentiated anticholinergic effects
CNS depressants: Increased CNS depression
MAO inhibitors: Possibly severe hypotension and prolonged and intensified anticholinergic and sedative effects of dexchlorpheniramine
alcohol use: Increased CNS depression

Side Efect

CNS: Ataxia, confusion, dizziness, drowsiness, euphoria, excitement, headache, insomnia, irritability, nervousness, neuritis, nightmares, paresthesia, restlessness, vertigo, weakness
CV: Hypotension, palpitations, tachycardia
EENT: Acute labyrinthitis, blurred vision, dry mouth, tinnitus, vision changes
GI: Anorexia, constipation, diarrhea, indigestion, nausea, vomiting
GU: Urinary hesitancy, urine retention
RESP: Tenacious bronchial secretions
SKIN: Diaphoresis, photosensitivity, rash

Cautions

Use dexchlorpheniramine cautiously in elderly patients and those with CV disease, hyperthyroidism, increased intraocular pressure, prostatic hypertrophy, or renal disease.

Monitor patient for

Side Efect

, especially in elderly patients and children.

Watch for evidence of overdose, including clumsiness; drowsiness; dry mouth, nose, or throat; dyspnea; flushed or red face; hallucinations; insomnia; light-headedness; seizures; and unsteadiness.

PATIENT SAFTY

Inform patient that drug provides tempodexchlorpheniramine maleate 301 D * For syrup and tablets; unknown for tablets. rary relief of symptoms.

Advise patient to take drug with food, water, or milk to reduce GI irritation. Inform her that she can crush regular (not ) tablets and mix with food or fluid.

For tablets, tell patient not to break, crush, or chew them before swallowing.

Urge patient to take missed dose as soon as possible unless it’s almost time for next dose.

Because drug may cause drowsiness, caution patient to avoid hazardous activities until its CNS effects are known.

Instruct her to avoid prolonged sun exposure and to use a sunscreen.

Suggest that patient use sugarless candy or gum, ice chips, or saliva substitute to relieve dry mouth. If dryness lasts longer than 2 weeks, urge her to notify prescriber.

Caution patient to avoid alcohol and CNS depressants, such as sedatives, sleepng pills, and tranquilizers, during therapy.

If patient takes high doses of aspirin, urge her to inform prescriber because antihistamines may mask

Side Efect

to aspirin overdose, such as tinnitus.

Inform patient that drug needs to be discontinued 3 to 4 days before skin tests for allergies are performed.

Category

Chemical class: d-threo-enantiomer of methylphenidate
Therapeutic class: CNS stimulant

Pregnancy category: C

Controlled substance schedule: II

Indications

To treat attention deficit hyperactivity disorder (ADHD) Adults and children age 6 and over who are new to methylphenidate.2.5 mg b.i.d. at least 4 hr apart, increased weekly by 2.5 to 5 mg. Maximum: 10 mg b.i.d. Adults and children age 6 and over who take methylphenidate. Half of racemic methylphenidate dosage. Maximum: 10 mg b.i.d. at least 4 hr apart.
DOSAGE ADJUSTMENT Drug stopped if no improvement within 1 mo after appropriate
DOSAGE ADJUSTMENTs. Dosage decreased or drug stopped for paradoxical aggravation of symptoms or

Side Efect

. , Adults who are new to methylphenidate. 10 mg daily, increased after 1 wk as needed to 20 mg daily. Children age 6 and over who are new to methylphenidate. 5 mg daily, increased weekly as needed by 5-mg increments. Maximum: 20 mg daily. Adults and children age 6 and over who take methylphenidate. Half of racemic methylphenidate dosage. Maximum: 20 mg daily.

Mechanism of Action

May block reuptake of norepinephrine and dopamine into presynaptic neurons in cerebral cortex, which increases availability of norepinephrine and dopamine in extraneuronal space.

Contraindications

Diagnosis or family history of Tourette’s syndrome; glaucoma; hypersensitivity to dexmethylphenidate, methylphenidate, or their components; marked anxiety, tension, and agitation; motor tics; use within 14 days of MAO inhibitor

Interactions

anticoagulants (oral), anticonvulsants, antidepressants (tricyclic and selective serotonin reuptake inhibitors): Possibly decreased metabolism of these antihypertensives: Decreased therapeutic effect of these dopamine and other vasopressors: Increased therapeutic effect of these
MAO inhibitors: Increased adverse effects, risk of hypertensive crisis

Side Efect

CNS: Cerebral arteritis or occlusion, dizziness, drowsiness, dyskinesia, fever, headache, insomnia, motor or vocal tics, nervousness, seizures, Tourette’s syndrome, toxic psychosis
CV: Angina, arrhythmias, hypertension, hypotension, increased or decreased pulse rate, palpitations, tachycardia dexmethylphenidate hydrochloride 302
EENT: Accommodation abnormality, blurred vision
GI: Abdominal pain, anorexia, nausea
HEME: Thrombocytopenic purpura
MS: Arthralgia
SKIN: Erythema multiforme, exfoliative dermatitis, necrotizing vasculitis, rash, urticaria
Other: Weight loss (prolonged therapy)

Cautions

WARNING Be aware that dexmethylphenidate may induce CNS stimulation, mania, and psychosis and may worsen behavior disturbances and thought disorders. Use drug cautiously in children with psychosis or mania. Be aware that withdrawal symptoms may occur with long-term use.

Also know that dexmethylphenidate should be used cautionly in patients with serious structural cardiac abnormalities, cardiomyopathy, serious heart rhythm abnormalities, or other serious cardiac problems because drug may increase risk of sudden death from these conditions.

Monitor blood pressure and pulse rate to detect hypertension and excessive stimulation. Notify prescriber if signs appear.

Dexmethylphenidate shouldn’t be used to treat severe depression or to prevent or treat normal fatigue.
WARNING Monitor patient for signs of physical or psychological dependence. Use drug cautiously in patients with a history of drug abuse, including alcoholism.

Monitor CBC and differential and platelet counts, as ordered, during prolonged therapy.

Expect to stop drug if seizures occur. Drug may lower seizure threshold, especially in patients with a history of seizures or EEG abnormalities.

Monitor children on long-term dexmethylphenidate therapy for signs of growth suppression, which has been noted during long-term use of stimulants.

Dosages of affected by dexmethylphenidate, such as anticoagulants and antihypertensives, may need adjustment.

PATIENT SAFTY

Tell patient that extended-release capsules should either be taken whole, without being chewed, crushed, or divided, or capsule contents should be sprinkled on a small amount of applesauce.

Urge patient to notify prescriber if she has excessive nervousness, fever, insomnia, nausea, palpitations, or rash while taking dexmethylphenidate.

Caution patient with seizure disorder that drug may cause seizures.

Advise patient to protect drug from light and moisture.

Teach patient (or parent) to watch for improvement in signs and symptoms of ADHD, such as decreased impulsiveness and increased attention. Stress the need for continued follow-up care, and suggest participation in an ADHD program.

Category

Chemical class: Piperazinedione
Therapeutic class: Cardioprotective agent, chelating agent

Pregnancy category: C

Indications

To prevent or reduce severity of cardiomyopathy related to doxorubicin therapy in women with metastatic breast cancer I.V. INJECTION
Adults.Initial: 500 mg/m2 for every 50 mg/ m2of doxorubicin every 3 wk.
DOSAGE ADJUSTMENT In patients with hyperbilirubinemia, dosage proportionately reduced (depending on severity) to maintain a dexrazoxane-to-doxorubicin ratio of 10:1. If creatinine clearance is less than 40 ml/min/1.73 m2, dosage decreased 50%.

Mechanism of Action

Rapidly enters cardiac cells and acts as an intracellular heavy metal chelator. In cardiac tissues, anthracyclines, such as doxorubicin, form complexes with iron or copper, damaging cardiac cell membranes and mitochondria. Dexrazoxane combines with intracellular iron and protects against anthracycline-induced free radical damage to the myocardium. It also prevents conversion of ferrous ions back to ferric ions for use by free radicals.

Incompatibilities

Don’t mix dexrazoxane in same I.V. line with other . dexrazoxane 303 D

Contraindications

Hypersensitivity to dexrazoxane or its components; use with chemotherapy regimens that do not contain an anthracycline, such as daunorubicin, doxorubicin, epirubicin, idarubicin, or mitoxantrone

Interactions

bone marrow depressants: Possibly enhanced bone marrow depression

Side Efect

HEME: Myelosuppression (granulocytopenia, leukopenia, thrombocytopenia)
Other: Injection site pain

Cautions

WARNING Use gloves when preparing reconstituted solution. If dexrazoxane powder or solution contacts your skin or mucosa, immediately and thoroughly wash with soap and water.

To reconstitute, mix with 25 or 50 ml of 0.167 molar sodium lactate, supplied by manufacturer, to produce 10 mg/ml. Give reconstituted solution by slow I.V. push, or further dilute with normal saline solution or D5W to 1.3 to 5 mg/ml, as prescribed, for rapid I.V. infusion.

Dexrazoxane may interfere with tumor response to doxorubicin, especially if given at start of fluorouracil-doxorubicincyclophosphamide therapy.

Monitor patient with immunosuppression or decreased bone marrow reserves from prior chemotherapy or radiation therapy to prevent worsening of her condition. Notify prescriber if condition deteriorates.

PATIENT SAFTY

Inform patient that dexrazoxane protects the heart from damage by myelosuppression and that she’ll be given the drug by a health care professional in the hospital or clinic before receiving chemotherapy.

Inform patient that dexrazoxane and chemotherapy may make her feel generally unwell, but urge her to continue treatment unless prescriber tells her to stop.

Instruct patient to report chills, fever, mouth sores, pain at injection site, sore throat, unusual bleeding or bruising, unusual tiredness or weakness, and vomiting. Dosage may need to be changed or therapy stopped.

Inform patient that drug may worsen symptoms of bone marrow suppression caused by anthracycline chemotherapy, including increased risk of infection.

Teach patient importance of avoiding injury and infection during dexrazoxane therapy. For example, advise her to use a soft-bristled toothbrush to prevent damage to teeth and gums; to avoid people with colds, flu, or bronchitis; and to avoid anyone who has recently had oral polio vaccine because of the increased risk of infection from live virus.

Category

Chemical class: Monosaccharide
Therapeutic class: Antidiabetic, nutritional supplement

Pregnancy category: C

Indications

To treat insulin-induced hypoglycemia CHEWABLE , ORAL GEL Adults and children.Initial: 10 to 20 g. Repeated in 10 to 20 min, if needed, based on serum glucose level.

IV

OR INJECTION Adults and children. Initial: 20 to 50 ml of 50% solution given at 3 ml/min. Maintenance: 10% to 15% solution by continuous infusion until blood glucose level reaches therapeutic range. Infants and neonates. 2 ml/kg of 10% to 25% solution until blood glucose level reaches therapeutic range. To replace calories
IV: Adults and children. Individualized dosage of 2.5%, 5%, or 10% solution, based on need for fluids or calories and given by peripheral I.V. line. Or 10% to 70% soludextrose 304 tion given by central vein, if needed, typically with amino acids or other solutions. Route Onset Peak Duration P.O. 10–20 min 40 min Unknown I.V. 2–3 min Unknown Unknown

Mechanism of Action

Prevents protein and nitrogen loss, promotes glycogen deposition, prevents or decreases ketosis, and, in large amounts, acts as an osmotic diuretic. Dextrose is readily metabolized and undergoes oxidation to carbon dioxide and water. The oral form—glucose—is absorbed directly into the bloodstream from the intestines and is distributed, used, or stored in the liver.

Incompatibilities

Don’t give dextrose through same infusion set as blood or blood products because pseudoagglutination of RBCs may occur.

Contraindications

For all solutions: Diabetic coma with excessively elevated blood glucose level For concentrated solutions: Anuria, alcohol withdrawal syndrome in dehydrated patient, glucose-galactose malabsorption syndrome, hepatic coma, hypersensitivity to corn or corn products, intracranial or intraspinal hemorrhage, overhydration

Interactions

corticosteroids, corticotropin: Increased risk of fluid and electrolyte imbalance if dextrose solution contains sodium ions

Side Efect

CNS: Confusion, fever
GU: Glycosuria
Other: Dehydration; hyperosmolar coma; hypervolemia; hypovolemia; injection site extravasation with tissue necrosis, infection, phlebitis, and venous thrombosis

Cautions

Use dextrose cautiously in patients with renal impairment because solutions contain aluminum that could be toxic in prolonged parenteral therapy.

Give highly concentrated dextrose solution by central venous catheter—not by subcutaneous or I.M. route.
WARNING Rapid or excessive delivery of dextrose solution in a very low–birthweight infant may increase serum osmolality and cause intracerebral hemorrhage.

Assess infusion site regularly for signs of infiltration, such as pain or swelling.

Assess patient for glucosuria by using a urine reagent strip or collecting a urine sample and reviewing urinalysis results.

When discontinuing a concentrated solution, expect to give a 5% to 10% dextrose infusion to avoid rebound hypoglycemia.

Monitor patient for signs of hypervolemia, such as jugular vein distention and crackles.

PATIENT SAFTY

Advise patient to swallow oral dextrose; it isn’t absorbed from the buccal cavity.

Instruct patient to monitor her blood glucose level as directed.

Stress importance of reporting discomfort, pain, or signs of infection at I.V. site.

Category

Chemical class: Aminotetralin, synthetic opioid
Therapeutic class: Analgesic

Pregnancy category: C

Indications

To relieve pain
I.V.INJECTION Adult.Initial: 5 mg followed by 2.5 to 10 mg every 2 to 4 hr, p.r.n. Maximum: 120 mg daily.
I.M.INJECTION Adult. Initial: 10 mg followed by 5 to 20 mg every 3 to 6 hr, p.r.n. Maximum: 20 mg/ dose, 120 mg daily. Route Onset Peak Duration I.V. In 15 min 30 min 2–4 hr I.M. In 30 min 1–2 hr 2–4 hr

Mechanism of Action

Binds with opiate receptors at many CNS sites, affecting perception of and emotional response to pain.

Contraindications

Hypersensitivity to dezocine or its components dezocine 305 D

Interactions

CNS depressants, general anesthetics, hypnotics, sedatives, tranquilizers: Increased CNS depressant effects opioids: Possibly decreased therapeutic opioid effects and withdrawal symptoms in patient receiving long-term opioid therapy
alcohol use: Increased CNS depression

Side Efect

CNS: Dizziness, sedation, vertigo
GI: Nausea, vomiting
Other: Injection site redness and swelling

Cautions

Use dezocine cautiously and in low doses in elderly patients and those who have common bile duct, hepatic, renal, or respiratory disease.

Discard solution if it contains precipitate.

Monitor blood pressure, pulse, and respiratory rate often after giving first dose, especially if given by I.V. route.
WARNING Avoid giving dezocine to opioiddependent patient. Doing so may precipitate withdrawal symptoms because dezocine can antagonize opioid effects.

Assess patient for pain relief often, and document findings.

PATIENT SAFTY

Instruct patient to notify prescriber if pain isn’t relieved within 1 hour.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Category

Chemical class: Benzodiazepine
Therapeutic class: Anticonvulsant, anxiolytic, sedative-hypnotic, skeletal muscle relaxant

Pregnancy category: D

Controlled substance schedule: IV

Indications

To relieve anxiety

ORALL

,
Adults.2 to 10 mg b.i.d. to q.i.d.
DOSAGE ADJUSTMENT Dosage reduced to 2 to 2.5 mg daily or b.i.d. and increased gradually as needed and tolerated for elderly or debilitated patients. Children age 6 months and over.Initial: 1 to 2.5 mg t.i.d. or q.i.d. Increased gradually as needed and tolerated. I.V.OR
I.M.INJECTION
Adults. 2 to 5 mg every 3 to 4 hr, p.r.n., for moderate anxiety; 5 to 10 mg every 3 to 4 hr, p.r.n., for severe anxiety. Children. Individualized dosage. Maximum: 0.25 mg/kg given over 3 min, repeated after 15 to 30 min if needed, and after another 15 to 30 min if needed. To treat symptoms of acute alcohol withdrawal

ORALL

,
Adults.10 mg t.i.d. or q.i.d. during first 24 hr. Then 5 mg t.i.d. or q.i.d., if needed. I.V.OR
I.M.INJECTION
Adults. 10 mg and then 5 to 10 mg in 3 to 4 hr, if needed. To provide muscle relaxation, to provide sedation

ORALL

,
Adults.2 to 10 mg t.i.d. or q.i.d.
DOSAGE ADJUSTMENT Dosage reduced to 2 to 2.5 mg once or twice daily and increased gradually as needed and tolerated for elderly or debilitated patients. Children age 6 months and over. Initial: 1 to 2.5 mg t.i.d. or q.i.d. Increased gradually as needed and tolerated. I.V.OR
I.M.INJECTION
Adults. 2 to 5 mg every 3 to 4 hr, p.r.n., for moderate anxiety; 5 to 10 mg every 3 to 4 hr, p.r.n., for severe anxiety. Children. Individualized dosage. Maximum: 0.25 mg/kg given over 3 min, repeated after 15 to 30 min if needed, and after another 15 to 30 min if needed. To treat seizures

ORALL

,
Adults.2 to 10 mg b.i.d. to q.i.d.
DOSAGE ADJUSTMENT Dosage reduced to 2 to 2.5 mg once or twice daily and increased gradually as needed and tolerated for elderly or debilitated patients. Children age 6 months and over. Initial: 1 to 2.5 mg t.i.d. or q.i.d. Increased gradually as needed and tolerated. To treat status epilepticus and severe recurrent seizures
I.V.INJECTION diazepam 306
Adults.5 to 10 mg repeated every 10 to 15 min, as needed, up to a cumulative dose of 30 mg. Regimen repeated, if needed, in 2 to 4 hr. (Use I.M. route if I.V. access is impossible.) Children age 5 and over. 1 mg repeated every 2 to 5 min, as needed, up to a cumulative dose of 10 mg. Regimen repeated, if needed, in 2 to 4 hr. Children ages 1 month to 5 years. 0.2 to 0.5 mg repeated every 2 to 5 min, as needed, up to a cumulative dose of 5 mg. Regimen repeated, if needed, in 2 to 4 hr. RECTAL GEL Adults and adolescents. 0.2 mg/kg rounded up to next available unit dose (or rounded down for elderly or debilitated patient). Repeated in 4 to 12 hr, if needed. Children ages 6 to 12. 0.3 mg/kg rounded up to next available unit dose. Repeated in 4 to 12 hr, if needed. Children ages 2 to 6. 0.5 mg/kg rounded up to next available unit dose. Repeated in 4 to 12 hr, if needed. To provide preoperative sedation I.V.OR
I.M.INJECTION
Adults.5 to 10 mg 30 min before surgery. To reduce anxiety before cardioversion
I.V.INJECTION
Adults. 5 to 15 mg 5 to 10 min before procedure. To reduce anxiety before endoscopic procedures
I.V.INJECTION
Adults.Up to 20 mg titrated to desired sedation and given immediately before procedure.
I.M.INJECTION
Adults. 5 to 10 mg 30 min before procedure. To treat tetanus I.V.OR
I.M.INJECTION Adults and children age 5 and over.Initial: 5 to 10 mg repeated every 3 to 4 hr, if needed. Sometimes larger doses for
Adults.
DOSAGE ADJUSTMENT Initial dose reduced to 2 to 5 mg and increased gradually as needed and tolerated for debilitated patients. Children ages 1 month to 5 years.1 to 2 mg repeated every 3 to 4 hr, as needed.

Mechanism of Action

May potentiate effects of gamma-aminobutyric acid (GABA) and other inhibitory neurotransmitters by binding to specific benzodiazepine receptors in limbic and cortical areas of CNS. GABA inhibits excitatory stimulation, which helps control emotional behavior. Limbic system contains a dense area of benzodiazepine receptors, which may explain drug’s antianxiety effects. Diazepam suppresses spread of seizure activity caused by seizure-producing foci in cortex, thalamus, and limbic structures.

Incompatibilities

Don’t mix diazepam injection with aqueous solutions. Don’t mix diazepam emulsion for I.M. injection with morphine or glycopyrrolate or administer it through an infusion set that contains polyvinyl chloride.

Contraindications

Acute angle-closure glaucoma, hypersensitivity to diazepam or its components, untreated open-angle glaucoma

Interactions

antacids: Altered rate of diazepam absorption anticonvulsants: Decreased effectiveness of these cimetidine, disulfiram, fluoxetine, fluvoxamine, isoniazid, itraconazole, ketoconazole, metoprolol, omeprazole, oral contraceptives, propoxyphene, propranolol,
valproic acid: Decreased diazepam metabolism, increased blood level and risk of adverse effects
CNS depressants: Increased CNS depression digoxin: Increased serum digoxin level and risk of digitalis toxicity levodopa: Decreased antidyskinetic effect of levodopa
phenytoin: Decreased metabolic elimination of phenytoin, increased risk of adverse reactions probenecid: Faster onset or more prolonged effects of diazepam ranitidine: Delayed elimination and increased blood level of diazepam
rifampin: Decreased blood diazepam level theophyllines: Antagonized sedative effect of diazepam
alcohol use: Increased CNS depression

Side Efect

CNS: Anterograde amnesia, anxiety, ataxia, confusion, depression, dizziness, drowsiness, fatigue, headache, insomnia, lethargy, lightheadedness, paradoxical reactions, psychidiazepam 307 D atric effects, sedation, sleepiness, slurred speech, suicidal ideation, tremor, vertigo
CV: Hypotension, palpitations, tachycardia
EENT: Blurred vision, diplopia, dry mouth, increased salivation
GI: Anorexia, constipation, diarrhea, elevated liver enzymes, jaundice, nausea, vomiting
GU: Libido changes, urinary incontinence, urine retention
HEME: Neutropenia
MS: Dysartrhia, muscle weakness
RESP: Respiratory depression
SKIN: Dermatitis
Other: Physical and psychological dependence

Cautions

Use diazepam with extreme caution in patients with a history of alcohol or drug abuse because it can cause physical and psychological dependence, and in patients with hepatic disorders such as hepatic fibrosis and hepatitis because of potentially significant increase in drug’s half-life.

Use diazepam cautiously in patients with hepatic or renal impairment. Severe hepatic impairment is a contraindication to use.

Expect to give a lower diazepam dose to patient with chronic respiratory insufficiency because of the risk of respiratory depression.

Mix concentrated oral solution (Intensol) with liquid or semisolid food. Use supplied calibrated dropper to measure doses.

Protect diazepam injection from light. Don’t use solution that’s more than slightly yellow or that contains precipitate.

Give I.M. injection into deltoid muscle for rapid, complete absorption. Using other sites may cause slow, erratic absorption.

Before administering emulsion form, ask if patient is allergic to soybeans because this form contains soybean oil.

For an infant or a child, administer I.V. injection slowly over 3 minutes in a dose not to exceed 0.25 mg/kg.

Give emulsion form within 6 hours of opening ampule because it contains no preservatives and allows rapid microbial growth. Use polyethylene-lined or glass infusion sets and polyethylene or polypropylene plastic syringes for administration. Don’t use a filter with a pore size less than 5 microns because a smaller size may break down the emulsion.

Don’t mix emulsion form with anything other than its emulsion base. Otherwise, it may become unstable and increase the risk of serious

Side Efect

.

Monitor patient for

Side Efect

, especially if she has hypoalbuminemia, which increases the risk of sedation.
WARNING Watch for signs of physical and psychological dependence (strong desire or need to continue taking diazepam, need to increase dose to maintain drug effects, and posttherapy withdrawal symptoms, such as abdominal cramps, insomnia, irritability, nervousness, and tremor).

Monitor patient closely for increase in frequency or severity of grand mal seizures when diazepam is used with standard anticonvulsant therapy. Dosage of other anticonvulsants may need to be increased.

Avoid abrupt withdrawal of diazepam, as ordered, when used as part of the patient’s seizure control regimen because a transient increase in frequency or severity of seizures may occur.

Monitor severely depressed patient or one with depression-related anxiety for suicidal tendencies, particularly when therapy starts and dosage changes; depression may worsen temporarily during these times.

Watch for psychiatric and paradoxical reactions to diazepam, especially in children and the elderly. If reations occur, notify prescriber and expect drug to be discontinued.

Monitor patient for decreased drug effectiveness, especially with prolonged use.

Check patient’s blood counts and liver function periodically, as ordered, because prolonged diazepam therapy rarely causes neutropenia and jaundice.

PATIENT SAFTY

Instruct patient not to take more drug, more often, or for a longer time than prescribed. Warn her that physical and psychological dependence can occur, and teach her to recognize the signs.

Advise patient not to take drug to relieve everyday stress.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to avoid CNS depressants and alcohol during therapy.

Instruct patient not to stop taking drug abruptly without prescriber’s supervision. diazepam 308 If patient has a history of seizures, warn that abrupt withdrawal may trigger them.

Instruct patient to mix Diazepam Intensol with water, soda, or a similar beverage; applesauce; or pudding just before taking it. Caution her not to save the mixture for later. Tell her to use calibrated dropper that’s provided to measure each dose.

Teach patient how to self-administer a rectal form, if prescribed.

Instruct female patient of childbearing age to notify prescriber immediately if she is or could be pregnant because diazepam therapy will need to be discontinued.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes.

Category

Chemical class: Benzothiadiazine derivative
Therapeutic class: Antihypertensive, antihypoglycemic

Pregnancy category: C

Indications

To manage hypoglycemia caused by hyperinsulinism , ORAL SUSPENSION Adults and children.Initial: 1 mg/kg every 8 hr. Maintenance: 3 to 8 mg/kg daily in 2 or 3 equal doses given every 8 or 12 hr. Maximum: 15 mg/kg daily. Infants and neonates.Initial: 3.3 mg/kg every 8 hr. Maintenance: 8 to 15 mg/kg daily in 2 or 3 equal doses given every 8 or 12 hr. To treat severe hypertension in hospitalized patients
I.V.INJECTION Adults and children.Initial: 1 to 3 mg/kg by rapid bolus, repeated every 5 to 15 min until diastolic pressure falls below 100 mm Hg. Repeated in 4 hr and again in 24 hr, if needed, until oral antihypertensive therapy begins. Maximum: 150 mg/dose, 1.2 g daily.

Mechanism of Action

Directly affects smooth muscle cells of peripheral arteries and arterioles, causing them to dilate. This action decreases peripheral resistance, which helps reduce blood pressure. Diazoxide also inhibits insulin release from the pancreas, stimulates catecholamine release, and increases hepatic glucose release. Route Onset Peak Duration P.O. In 1 hr Unknown 8 hr I.V. 1 min 2–5 min 2–12 hr

Contraindications

Acute aortic dissection; hypersensitivity to diazoxide, thiazides, other sulfonamide derivatives, or their components; treatment of compensatory hypertension, as occurs with aortic coarctation

Interactions

allopurinol, colchicine, probenecid, sulfinpyrazone: Increased serum uric acid level antihypertensives: Additive hypotensive effects
beta blockers: Increased hypotensive effects of diazoxide diuretics, especially thiazides: Potentiated hyperglycemic, hyperuricemic, and antihypertensive effects of diazoxide estrogens, NSAIDs, sympathomimetics: Antagonized diazoxide hypotensive effects insulin, oral antidiabetics: Possibly decreased effectiveness of these oral anticoagulants: Increased anticoagulation peripheral vasodilators, ritodrine (I.V.): Additive, possibly severe, hypotensive effects

Side Efect

CNS: Anxiety, apprehension, cerebral ischemia, dizziness, euphoria, headache, insomnia, light-headedness, malaise, somnolence, weakness
CV: Bradycardia, chest pain, hypotension, palpitations, tachycardia, transient hypertension
EENT: Blurred vision, dry mouth, increased salivation, taste perversion, tinnitus, transient hearing loss
ENDO: Transient hyperglycemia
GI: Abdominal pain, anorexia, constipation, diarrhea, ileus, nausea, vomiting
MS: Gout
SKIN: Diaphoresis, flushing, pruritus, rash, sensation of warmth
Other: Extravasation with injection site cellulitis and pain; fluid and sodium retention diazoxide 309 D

Cautions

Use diazoxide cautiously in patients with uncompensated heart failure (can cause fluid retention and heart failure) and patients with impaired cardiac or cerebral circulation in whom abrupt blood pressure drop, mild tachycardia, and decreased blood perfusion may be harmful.

Give I.V. drug undiluted over 10 to 30 seconds. Don’t give it I.M. or subcutaneously.

Keep patient supine during I.V. injection and for 1 hour afterward.

Monitor blood pressure throughout treatment to check for hypertension. Before monitoring ends, measure patient’s standing blood pressure if she’s ambulatory.

Assess I.V. site often for extravasation; drug is alkaline and can irritate tissue.

Expect to adjust dosage if patient switches from oral suspension to capsules; suspension causes a higher blood diazoxide level.

If diabetic patient receives I.V. diazoxide to treat hypertension, watch for evidence of hyperglycemia because parenteral form commonly causes transient hyperglycemia.

Monitor blood glucose level of all patients who receive oral diazoxide to see if drug has raised blood glucose level to normal.

PATIENT SAFTY

Tell patient who receives I.V. diazoxide that she’ll be on bed rest until taking oral drug.

Advise patient to protect oral suspension from light.

Tell patient to take oral drug on a regular schedule and not to skip or double doses.

Urge patient to monitor blood glucose level if she takes oral drug for hypoglycemia.

Caution patient not to take antidiabetic unless prescribed.

Advise patient to notify prescriber if she has signs of hyperglycemia, such as increased urinary frequency, increased thirst, and fruity breath.

Category

Chemical class: Sympathomimetic amine
Therapeutic class: Analgesic

Pregnancy category: Not rated

Indications

To relieve tension headache
Adults.1 to 2 caps every 4 hr. Maximum: 8 capsules daily. To relieve migraine headache
Adults. 2 caps followed by 1 cap every hr until relief occurs. Maximum: 5 capsules every 12 hr. Route Onset Peak Duration P.O. 30–60 min 1–3 hr 3–4 hr

Mechanism of Action

Dichloralphenazone reduces emotional reaction to pain through mild sedative effect. Acetaminophen raises pain threshold by acting on hypothalamus. Isometheptene constricts dilated cranial and cerebral arterioles through sympathomimetic action, reducing stimuli for vascular headaches.

Contraindications

Heart disease, hepatic disease, hypersensitivity to acetaminophen or isometheptene, MAO inhibitor therapy within 14 days, severe renal disease, uncontrolled glaucoma, uncontrolled hypertension

Interactions

CNS depressants: Additive sedative effects hepatic enzyme inducers, other hepatotoxic : Increased risk of hepatotoxicity
MAO inhibitors: Increased risk of severe hypertension and hyperpyrexia
alcohol use: Additive sedative effects, increased risk of hepatotoxicity

Side Efect

CNS: Dizziness, drowsiness
SKIN: Rash

Cautions

Because dichloralphenazone has vasoconstrictive and sympathomimetic actions, assess patients with peripheral vascular disease or recent angina pectoris or MI for signs and symptoms indicating aggravadichloralphenazone 310 tion or deterioration of these conditions.

Institute safety precautions to prevent injury from falls.

PATIENT SAFTY

WARNING Caution patient not to take dichloralphenazone within 14 days of an MAO inhibitor; doing so can cause severe hypertension or hyperpyrexia.

Advise patient to take drug only after a headache or migraine
WARNING sign occurs. Too-frequent use may make drug less effective and may worsen headaches.

Instruct patient to lie down in a quiet, dark room after taking drug.

Because of possible dizziness or drowsiness, caution patient to avoid hazardous activities until drug’s CNS effects are known.

Caution patient to avoid alcohol and CNS depressants during therapy because they increase dizziness, drowsiness, and the risk of hepatotoxicity.

Advise patient to notify prescriber if drug becomes less effective or if headaches occur more often.

Teach patient how to read drug labels and avoid taking too much acetaminophen, which can cause hepatic or renal damage.

Explain that decreasing dichlralphenazone dose may prevent dizziness or rash.

Instruct patient to store drug away from heat, moisture, and direct light.

Category

Chemical class: Sulfonamide derivative
Therapeutic class: Antiglaucoma drug

Pregnancy category: C

Indications

To manage chronic open-angle glaucoma, secondary glaucoma, and acute angle-closure glaucoma (preoperatively)
Adults.Initial: 100 to 200 mg followed by 100 mg every 12 hr. Maintenance: 25 to 50 mg once daily to t.i.d.

Mechanism of Action

Inhibits the enzyme carbonic anhydrase, which normally is in renal proximal tubule cells, choroid plexes of the brain, and ciliary processes of the eyes. In eyes, enzyme inhibition decreases aqueous humor secretion, which reduces intraocular pressure. Route Onset Peak Duration P.O. 30–60 min 2–4 hr 6–12 hr

Contraindications

Adrenocortical insufficiency, hepatic insufficiency, hyperchloremic acidosis, hypersensitivity to dichlorphenamide or sulfa , hypokalemia, hyponatremia, renal failure, severe obstructive pulmonary disease

Interactions

diflunisal: Increased adverse effects of dichlorphenamide, significantly decreased intraocular pressure salicylates: Increased risk of dichlorphenamide toxicity, including CNS depression and metabolic acidosis

Side Efect

CNS: Depression, disorientation, dizziness, drowsiness, lassitude, paresthesia
CV: Arrhythmias
EENT: Metallic taste, pharyngitis
ENDO: Hyperglycemia
GI: Anorexia, diarrhea, hepatic dysfunction, nausea, vomiting
GU: Phosphaturia, renal calculi, renal colic, urinary frequency
HEME: Hemolytic anemia, leukopenia, pancytopenia, thrombocytopenia
SKIN: Photosensitivity
Other: Hyperchloremia, hyperuricemia, weight loss

Cautions

Use dichlorphenamide cautiously in patients with emphysema, pulmonary obstruction, or severe respiratory acidosis.

Monitor serum potassium level often (especially in elderly patients and those taking digoxin) because diuresis may cause hypokalemia.

PATIENT SAFTY

Instruct patient to take dichlorphenamide with food or full glass of water to decrease GI distress.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.
WARNING Urge patient to immediately dichlorphenamide 311 D report evidence of blood dyscrasias, such as fever, numbness or tingling, rash, sore throat, and unusual bleeding or bruising.

Advise patient to avoid prolonged exposure to sunlight, to apply sunscreen, and to wear protective clothing outdoors.

Instruct patient to take a missed dose as soon as she remembers it, unless it’s almost time for the next dose.

Tell patient to store drug at room temperature and protect from moisture and heat.

Category

Chemical class: Phenylacetic acid derivative
Therapeutic class: Analgesic, antiinflammatory

Pregnancy category: B

Indications

To relieve pain and inflammation in rheumatoid arthritis DELAYED-RELEASE ,
Adults. Initial: 150 to 200 mg daily in divided doses t.i.d. or q.i.d. Maintenance: 75 to 100 mg/ day, divided, t.i.d. Maximum: 225 mg daily.
Adults. Initial: 75 or 100 mg daily, morning or evening, or 75 mg b.i.d., morning and evening. RECTAL SUPPOSITORIES
Adults. 50 or 100 mg as substitute for last P.O. dose of day. To relieve pain and inflammation in osteoarthritis DELAYED-RELEASE ,
Adults. 100 to 150 mg daily in divided doses b.i.d. or t.i.d. Maximum: 150 mg daily. To relieve pain in patients with ankylosing spondylitis DELAYED-RELEASE ,
Adults. 100 to 125 mg daily in 4 or 5 divided doses. To relieve pain and dysmenorrhea
Adults. 50 mg t.i.d., p.r.n.; if needed, 100 mg for first dose only.
DOSAGE ADJUSTMENT Dosage reduced, if needed, for elderly patients and those with serious renal dysfunction. To relieve mild to moderate acute pain
Adults.25 mg four times daily. Route Onset Peak Duration P.O.* 30 min Unknown 8 hr

Mechanism of Action

Blocks the activity of cyclooxygenase, the enzyme needed to synthesize prostaglandins, which mediate inflammatory response and cause local pain, swelling, and vasodilation. By blocking cyclooxygenase and inhibiting prostaglandins, diclofenac reduces inflammatory symptoms. This mechanism also relieves pain because prostaglandins promote pain transmission from periphery to spinal cord.

Contraindications

Active GI bleeding or ulcers; asthma attacks, rhinitis, or urticaria from aspirin or other NSAIDs; hypersensitivity to diclofenac or NSAIDs; treatment of perioperative pain after coronary artery bypass grafting

Interactions

acetaminophen: Increased risk of adverse renal effects with long-term concurrent use anticoagulants, thrombolytics: Prolonged PT, increased risk of bleeding antihypertensives: Decreased antihypertensive effectiveness aspirin, other NSAIDs, salicylates: Increased GI irritability and bleeding, decreased diclofenac effectiveness
beta blockers: Impaired antihypertensive effect cefamandole, cefoperazone, cefotetan, plicamycin,
valproic acid: Increased risk of hypoprothrombinemia
cimetidine: Altered blood diclofenac level colchicine, corticotropin (long-term use), glucocorticoids, potassium supplements: diclofenac 312 * For tablets; unknown for delayed-release and tablets. Increased GI irritability and bleeding cyclosporine, gold compounds, nephrotoxic : Increased risk of nephrotoxicity digoxin: Increased blood digoxin level insulin, oral antidiabetics: Decreased effects of these lithium: Increased risk of lithium toxicity loop diuretics: Decreased diuretic effects methotrexate: Increased risk of methotrexate toxicity
phenytoin: Increased blood phenytoin level potassium-sparing diuretics: Increased risk of hyperkalemia probenecid: Increased diclofenac toxicity food: Delayed absorption of delayed-release tablets
alcohol use: Increased risk of GI irritability and bleeding

Side Efect

CNS: Aseptic meningitis, cerebral hemorrhage, dizziness, drowsiness, headache
CV: Bradycardia and other arrhythmias, hypotension, vasculitis
EENT: Glaucoma, hearing loss, tinnitus
ENDO: Hypoglycemia
GI: Abdominal pain, constipation, diarrhea, dysphagia, elevated liver function test results, esophageal ulceration, flatulence, GI bleeding or ulceration, hepatic failure, hepatitis, indigestion, jaundice, nausea, perforation of stomach or intestine
GU: Acute renal failure, interstitial nephritis
HEME: Agranulocytosis, aplastic anemia, eosinophilia, leukocytosis, leukopenia, pancytopenia, porphyria, thrombocytopenia
SKIN: Erythema multiforme, exfoliative dermatitis, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, angioedema, fluid retention, hyperkalemia, hyperuricemia, hyponatremia, lymphadenopathy

Cautions

Use diclofenac with extreme caution and for shortest possible time in patients with a history of GI bleeding or ulcer disease because NSAIDs increase risk of GI bleeding and ulceration.

Don’t substitute one form of oral diclofenac for another. Different formulations aren’t bioequivalent.

Be aware that serious GI tract ulceration and bleeding, as well as perforation of stomach or intestine, can occur without
WARNING or symptoms. Elderly patients are at greater risk. Monitor patient for signs of GI irritation and ulceration, especially if patient has a predisposing condition (such as a history of GI bleeding); takes an oral corticosteroid, anticoagulant, or NSAID (long-term); smokes; is an alcoholic; is over age 60; has poor general health; or tests positive for Helicobacter pylori. To minimize risk, give diclofenac with food. If patient develops GI distress, withhold drug and notify prescriber immediately.

Use diclofenac cautiously in patients with hypertension, and monitor blood pressure closely; drug can cause or worsen hypertension.

Assess patient for hypotension. If patient takes a potassium-sparing diuretic, check for elevated serum potassium level.
WARNING Monitor patient closely for thrombotic events, including MI and stroke, because NSAIDs such as diclofenac increase the risk for such events.

Report signs of bleeding, such as bleeding gums, bloody or cloudy urine, ecchymoses, melena, and petechiae.

Monitor BUN and serum creatinine levels in elderly patients, patients taking ACE inhibitors or diuretics, and patients with heart failure or impaired renal or hepatic function. These patients may have an increased risk of renal failure.

Assess patient’s skin routinely for rash or other signs of hypersensitivity reaction; drug may cause serious skin reactions without
WARNING. At first sign of reaction, stop drug and notify prescriber.

Because severe hepatic reactions may occur during diclofenac therapy, monitor liver function test results and serum uric acid level. Liver enzyme elevations usually occur within 2 months of starting drug and should be reported promptly because dosage may need adjustment. Also monitor patient for evidence of hepatic dysfunction (diarrhea, fatigue, flulike symptoms, jaundice, lethargy, nausea, pruritus, right upper quadrant tenderness).

Report weight gain of more than 1 kg (2 lb) in 24 hours because it suggests fluid retention.

PATIENT SAFTY

diclofenac 313 D

Advise patient not to chew, crush, or dissolve tablet, but to swallow it whole.

Instruct patient to take diclofenac with food to minimize GI distress.

To decrease risk of esophageal ulceration, instruct patient not to lie down for 15 to 30 minutes after taking drug.

Warn patient to avoid hazardous activities until diclofenac’s CNS effects are known.

Urge patient to notify prescriber about ringing or buzzing in ears, impaired hearing, dizziness, or GI distress or bleeding.

Advise patient to consult prescriber before taking aspirin or other OTC analgesics or drinking alcohol.

Explain that diclofenac may increase risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention for signs and symptoms such as chest pain, shortness of breath, weakness, and slurred speech.

Tell patient that diclofenac also may increase risk of serious adverse GI reactions; stress need to seek immediate medical attention for such evidence as epigastric or abdominal pain, indigestion, black or tarry stools, and vomiting blood or material that looks like coffee grounds.

Alert patient about possibly serious skin reactions and need to seek immediate medial attention for such as problems as blisters, fever, itching, rash, and other signs of hypersensitivity.

Urge patient to promptly report adverse effects (nausea, fatigue, lethargy, diarrhea, pruritus, jaundice, right upper quadrant discomfort, flulike symptoms).

Category

Chemical class: Isoxazolyl penicillin derivative
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat mild to moderate upper respiratory tract and localized skin and softtissue infections caused by penicillinaseproducing staphylococci , Adults and children weighing 40 kg (88 lb) or more. 125 mg every 6 hr. Children weighing less than 40 kg. 12.5 mg/kg daily divided into four equal doses and given every 6 hr. To treat severe infections, such as lower respiratory tract or disseminated infections, caused by penicillinase-producing staphylococci , Adults and children weighing 40 kg or more.250 mg every 6 hr, or higher doses, if needed. Maximum: 6 g daily. Children over age 1 month weighing less than 40 kg. 25 mg/kg daily divided into 4 equal doses and given every 6 hr, or higher doses if needed.

Mechanism of Action

Inhibits cell wall synthesis in susceptible bacteria, which assemble rigid, cross-linked cell walls in several steps. Dicloxacillin affects final cross-linking by inactivating penicillin-binding protein (the enzyme needed to link cell wall strands). This action inhibits cell wall synthesis and causes cell lysis and death.

Contraindications

Hypersensitivity to dicloxacillin, other penicillins, beta-lactamase inhibitors (such as piperacillin/tazobactam), cephalosporins, imipenem, or their components

Interactions

hepatotoxic : Increased risk of hepatotoxicity methotrexate: Decreased methotrexate clearance and increased risk of toxicity oral contraceptives: Decreased contraceptive action probenecid: Increased and prolonged blood dicloxacillin level tetracyclines: Decreased dicloxacillin effectiveness all : Possibly delayed absorption

Side Efect

CNS: Dizziness, fatigue, fever, insomnia
EENT: Black “hairy”tongue, dry mouth, glossitis, laryngeal edema, laryngospasm, stomatitis, taste perversion
GI: Abdominal pain, anorexia, diarrhea, flatulence, nausea, pseudomembranous dicloxacillin sodium 314 colitis, transient hepatitis, vomiting
GU: Nephropathy, vaginitis
MS: Prolonged muscle relaxation
SKIN: Dermatitis, erythema multiforme, pruritus, rash, urticaria, vesicular eruptions
Other: Anaphylaxis, serum sicknesslike reaction, superinfection

Cautions

Before dicloxacillin therapy begins, expect to obtain body fluid and tissue samples for culture and sensitivity tests, as ordered, and review the results, if possible. Also check for history of sensitivity to cephalosporins, penicillins, and other substances.

If diarrhea develops, notify prescriber; it could be the development of pseudomembranous colitis.

PATIENT SAFTY

Instruct patient to take drug 1 hour before or 2 hours after meals.

Instruct patient to take drug around the clock, not to miss a dose, and to complete the entire prescription unless directed otherwise by prescriber.

Advise patient to take oral solution with a cold beverage but not acidic juice, such as orange juice. Explain that solution is effective for 7 days at room temperature and for 14 days if refrigerated.

Caution patient not to open capsules and mix contents with food or liquids because an unpleasant taste and decreased drug absorption will result.

Instruct parent to shake oral solution thoroughly and measure doses with a calibrated device for accuracy.

Advise patient to notify prescriber if she experiences adverse GI reactions or signs of hypersensitivity or superinfection.

If patient takes an oral contraceptive, advise her to use an additional form of contraception during therapy.

Instruct patient to store drug away from heat, moisture, and direct light and to refrigerate—but not freeze—oral solution.

Category

Chemical class: Coumarin derivative
Therapeutic class: Anticoagulant

Pregnancy category: X

Indications

To prevent and treat pulmonary embolus, thromboembolus, and venous thrombus; to prevent thromboembolism related to atrial fibrillation and mechanical heart valves
Adults. Initial: 200 to 300 mg on the first day. Maintenance: 25 to 200 mg daily.
DOSAGE ADJUSTMENT Dosage reduced for elderly patients and those with hepatic or renal impairment. Route Onset Peak Duration P.O. 1–5 days Unknown 5–6 days

Mechanism of Action

Prevents coagulation by interfering with the liver’s ability to synthesize vitamin K–dependent clotting factors. This in turn depletes clotting factors II (prothrombin), VII, IX, and X. Normally, clots result from a cascade of proteolytic reactions that involve several clotting factors, including vitamin K–dependent factors. These clotting factors must be converted to an activated form before the clotting cascade can continue. By depleting vitamin K–dependent clotting factors, dicumarol interferes with the clotting cascade and prevents coagulation.

Contraindications

Active bleeding; aneurysm; ascorbic acid deficiency; bacterial endocarditis; blood dyscrasia; continuous tube drainage of small intestine; diverticulitis; eclampsia or preclampsia; emaciation; hemophilia; hemorrhagic tendency; history of bleeding diathesis or warfarin-induced necrosis; leukemia; major regional lumbar block anesthesia; malnutrition; pericardial effusion; pericarditis; polyarthritis; pregnancy; prostatectomy; recent surgery on brain, eye, GI tract, or prostate; recovery from spinal puncture; severe hepatic or renal impairment; stroke; surgery resulting in large, open surfaces; threatened abortion; thrombocytopenic purpura; uncontrolled or malignant hypertension; visceral cancer; vitamin K deficiency

Interactions

acetaminophen, androgens, beta blockers, chlorpropamide, clofibrate, corticosteroids, dicumarol 315 D cyclophosphamide, dextrothyroxine, disulfiram, erythromycin, fluconazole, gemfibrozil, glucagon, hydantoins, influenza virus vaccine, isoniazid, ketoconazole, miconazole, moricizine, propoxyphene, quinolones, streptokinase, sulfonamides, tamoxifen, thioamines, thyroid , urokinase: Increased effects of dicumarol and risk of bleeding

Side Efect

CNS: Fever, malaise
ENDO: Adrenal hemorrhage
GI: Abdominal cramps and distention, anorexia, diarrhea, flatulence, nausea, vomiting
GU: Menorrhagia, priapism
HEME: Hemorrhage, leukopenia
SKIN: Alopecia, pruritus, rash, urticaria
Other: Allergic reaction, purple toes syndrome

Cautions

Use dicumarol cautiously in elderly patients and those with hepatic or renal impairment.

Monitor results of serial PT and INR tests, and expect to adjust dosage accordingly.

If patient also receives heparin, expect heparin therapy to continue until INR reaches desired level: 2 to 3 times the control value for pulmonary embolus, thromboembolus, or venous thrombus; or 3 to 4.5 times the control value for thromboembolism related to atrial fibrillation or mechanical valves.

If PT or INR are prolonged, withhold one dicumarol dose, as prescribed, and, to reverse anticoagulation, give vitamin K. If patient has severe bleeding, expect to give blood to offset vitamin K’s delayed onset.

Assess patient for signs of hemorrhage, such as ecchymosis, epistaxis, gingival bleeding, hematuria, and melena.

To reduce bleeding, apply pressure to I.M. or venipuncture sites for up to 5 minutes.

PATIENT SAFTY

Instruct patient to take dicumarol at the same time every day.

Inform patient that drug’s full effects may not occur for 2 to 7 days.

Instruct patient to have frequent coagulation tests, as prescribed.

Advise patient to stabilize her intake of high in vitamin K. Urge her to consult prescriber before starting a weightloss diet, altering eating habits, or taking new vitamins or other nutritional supplements; these activities may alter her vitamin K intake.

Caution patient to avoid activities that may cause bleeding. Advise the use of a soft toothbrush and an electric razor.

Urge patient to consult prescriber before taking OTC , including herbs; they may affect anticoagulant effect.

Instruct patient to take a missed dose as soon as she remembers unless it’s nearly time for the next dose. Urge her to report missed doses to prescriber.

Caution patient to immediately notify prescriber if signs of bleeding occur, such as abdominal pain or swelling; back pain; bloody or black stools; bloody urine; coughing up blood; joint pain, swelling, or stiffness; severe or continuing headache; and vomiting blood or material that looks like coffee grounds.

Urge patient to carry medical identification and tell all health care providers that she takes dicumarol.

Explain that coagulation will gradually return to normal after therapy stops. Remind patient to keep watching for bleeding.

Category

Chemical class: Tertiary amine
Therapeutic class: Anticholinergic, antispasmodic

Pregnancy category: Not rated

Indications

To control diarrhea and GI tract spasms , Adults and adolescents. 10 to 20 mg t.i.d. or q.i.d., increased as needed and tolerated. Maximum: 160 mg daily. Children ages 6 to 12. 10 mg t.i.d. or q.i.d. Adults and adolescents.30 mg b.i.d. SYRUP Adults and adolescents.10 to 20 mg t.i.d. or q.i.d., increased as needed and tolerated. dicyclomine hydrochloride 316 Maximum: 60 mg daily. Children ages 2 to 13. 10 mg t.i.d. or q.i.d. Children ages 6 months to 2 years. 5 to 10 mg t.i.d. or q.i.d.
I.M.INJECTION
Adults.20 mg every 4 to 6 hr. Dosage adjusted as needed and tolerated.

Mechanism of Action

Inhibits acetylcholine’s muscarinic actions at postganglionic parasympathetic receptors in smooth muscles, secretory glands, and the CNS. These actions relax smooth muscles and diminish GI, GU, and biliary tract secretions.

Contraindications

Adhesions between iris and lens, angleclosure glaucoma, GI obstruction, hemorrhagic shock, hepatic disease, hiatal hernia, hypersensitivity to any anticholinergic, ileus, intestinal atony in elderly or debilitated patients, myasthenia gravis, myocardial ischemia, obstructive uropathy, renal disease, severe ulcerative colitis, tachycardia, toxic megacolon

Interactions

adsorbent antidiarrheals, antacids: Decreased dicyclomine absorption amantadine, anticholinergics, phenothiazines, tricyclic antidepressants: Increased dicyclomine effects antimyasthenics: Reduced intestinal motility atenolol: Increased atenolol effects cyclopropane: Risk of ventricular arrhythmias
haloperidol: Decreased antipsychotic effect of haloperidol
ketoconazole: Decreased ketoconazole absorption metoclopramide: Decreased effect of metoclopramide on GI motility opioid analgesics: Increased risk of ileus, severe constipation, and urine retention potassium chloride, especially wax-matrix preparations: Possibly GI ulceration urinary alkalinizers (antacids that contain calcium or magnesium, carbonic anhydrase inhibitors, citrates, sodium bicarbonate): Delayed excretion and increased risk of adverse effects of dicyclomine

Side Efect

CNS: Agitation, dizziness, drowsiness, dyskinesia, excitement, fever, insomnia, lethargy, light-headedness (I.M. use), nervousness, paresthesia, syncope
CV: Palpitations, tachycardia
EENT: Blurred vision, cycloplegia, dry mouth, loss of taste, mydriasis, nasal congestion, photophobia
GI: Constipation, dysphagia, heartburn, ileus, vomiting
GU: Impotence, urine retention
SKIN: Decreased sweating, flushing, pruritus
Other: Heatstroke; injection site pain, redness, and swelling

Cautions

Assess patient for tachycardia before giving dicyclomine; heart rate may increase.

Don’t give drug by I.V. route.

Watch for symptoms of hypersensitivity, such as agitation and pruritus. They usually resolve within 48 hours of stopping drug.

During long-term use, assess patient for chronic constipation and fecal impaction, and take corrective measures, as prescribed.

PATIENT SAFTY

Instruct patient to store dicyclomine in a tightly sealed container at room temperature, protected from moisture and direct light. Advise her not to refrigerate syrup.

Inform patient that dicyclomine relieves symptoms but doesn’t cure the disorder.

For best results, instruct patient to take drug 30 to 60 minutes before eating.

Advise patient not to take an antacid or an anti-diarrheal within 2 hours of dicyclomine.

Inform patient that blurred vision, dizziness, or drowsiness may occur.

To prevent constipation, advise patient to eat high-fiber and drink at least eight glasses of water daily.
WARNING Urge patient to avoid getting overheated during exercise or in hot weather because heatstroke may result. Inform patient that hot baths or saunas may cause dizziness or fainting.

Instruct patient to change position slowly to avoid light-headedness.

Inform patient that stopping drug abruptly may cause dizziness and vomiting.

Tell patient to take a missed dose as soon as she remembers unless it’s nearly time for the next dose. Caution against doubling the dose.

Category

Chemical class: Difluorophenyl, salicylic acid derivative
Therapeutic class: Analgesic, antiinflammatory

Pregnancy category: C

(first trimester), Not rated (later trimesters)

Indications

To relieve mild to moderate pain
Adults. 1 g followed by 0.5 g every 8 to 12 hr. Maximum: 1.5 g daily. To reduce inflammation in osteoarthritis or rheumatoid arthritis
Adults. 0.5 to 1 g daily in divided doses b.i.d. Maximum: 1.5 g daily.
DOSAGE ADJUSTMENT Dosage reduced for elderly patients and those who use diuretics; who could be harmed by prolonged bleeding time; or who have compromised cardiac function, conditions that cause fluid retention, hepatic or renal impairment, hypertension, or upper GI disease. Route Onset Peak Duration P.O.* 1 hr 2–3 hr 8–12 hr

Mechanism of Action

Blocks the activity of cyclooxygenase, the enzyme needed to synthesize prostaglandins, which mediate the inflammatory response and cause local vasodilation, swelling, and pain. By blocking cyclooxygenase and inhibiting prostaglandins, this NSAID reduces inflammatory symptoms. This mechanism also relieves pain because prostaglandins promote pain transmission from the periphery to the spinal cord.

Contraindications

Asthma attacks, rhinitis, or urticaria precipitated by aspirin or other NSAIDs; hypersensitivity to diflunisal; treatment of perioperative pain after coronary artery bypass graft surgery

Interactions

acetaminophen: Increased risk of adverse renal effects with long-term use of both antacids: Decreased blood diflunisal level antihypertensives: Decreased antihypertensive effects aspirin, other NSAIDs, salicylates: Increased GI irritability and bleeding, decreased diflunisal effectiveness
beta blockers: Impaired antihypertensive effects of beta blocker cefamandole, cefoperazone, cefotetan, plicamycin,
valproic acid: Increased risk of hypoprothrombinemia colchicine, corticotropin (long-term use), glucocorticoids, potassium supplements: Increased GI irritability and bleeding cyclosporine, gold compounds, nephrotoxic : Increased risk of nephrotoxicity digoxin: Increased blood digoxin level heparin, oral anticoagulants, thrombolytics: Prolonged PT, increased risk of bleeding hydrochlorothiazide: Increased blood hydrochlorothiazide level insulin, oral antidiabetics: Increased hypoglycemic effects loop diuretics: Decreased loop diuretic effectiveness methotrexate: Increased risk of methotrexate toxicity
phenytoin: Increased blood phenytoin level probenecid: Increased diflunisal toxicity
alcohol use: Increased GI irritability and bleeding

Side Efect

CNS: Aseptic meningitis, cerebral hemorrhage, dizziness, drowsiness, headache, insomnia
CV: Vasculitis
EENT: Tinnitus
ENDO: Hypoglycemia
GI: Abdominal pain, constipation, diarrhea, esophageal irritation, GI bleeding or ulceration, hepatic failure, hepatitis, indigestion, jaundice, nausea, perforation of stomach or intestine, vomiting
GU: Acute renal failure, interstitial nephritis
HEME: Agranulocytosis, aplastic anemia, leukopenia, pancytopenia, thrombocytopenia
SKIN: Erythema multiforme, exfoliative diflunisal 318 * For analgesia; unknown for anti-inflammatory effects. dermatitis, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, angioedema, hyponatremia

Cautions

Use diflunisal with extreme caution and for shortest time possible in patients with a history of GI bleeding or ulcer disease because NSAIDs such as diflunisal increase the risk.

Serious GI tract ulceration and bleeding, as well as perforation of stomach or intestine, can occur without
WARNING or symptoms. Elderly patients are at greater risk. To minimize risk, give diflunisal with food. If patient has GI distress, withhold drug and notify prescriber immediately.

Use diflunisal cautiously in patients with hypertension, and monitor blood pressure closely during therapy; drug can cause or worsen hypertension.

Use drug cautiously in elderly patients, those with renal dysfunction, and those who should avoid prolonged bleeding time.
WARNING Monitor patient closely for thrombotic events, including stroke and MI, because NSAIDs such as diflunisal increase the risk of these events.

Monitor BUN and serum creatinine levels in elderly patients, patients taking ACE inhibitors or diuretics, and patients with heart falure or impaired hepatic or renal function. These patients may have an increased risk of renal failure.

Assess patient’s skin routinely for rash or other signs of hypersensitivity reaction; drug may cause serious skin reactions without
WARNING. At first sign of reaction, stop drug and notify prescriber.

Assess type, location, and intensity of pain before and 1 to 2 hours after giving drug.

Assess patient carefully because long-term or high-dose therapy may mask fever.

PATIENT SAFTY

Teach patient not to crush or chew diflunisal tablets.

Instruct patient to take tablet with a full glass of water and not to lie down for 30 minutes afterward to avoid esophageal irritation.

Inform patient that drug will start working in about 1 week but that full effects may not occur for several weeks.

Explain that diflunisal may increase the risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention for such signs and symptoms as chest pain, shortness of breath, slurred speech, and weakness.

Tell patient that diflunisal also may increase risk of serious adverse GI reactions; stress need to seek immediate medical attention for signs and symptoms such as abdominal or epigastric pain, black or tarry stools, indigestion, and vomiting blood or material that resembles coffee grounds.

Alert patient about possibly serious skin reactions and the need to seek immediate medial attention for such as problems as blisters, fever, itching, rash, and other signs of hypersensitivity.

Caution patient to avoid acetaminophen, alcohol, aspirin, and other salicylates during diflunisal therapy, unless directed otherwise by prescriber.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to tell health care providers about diflunisal therapy before surgery, including dental surgery. Therapy should stop for 1 week before procedure.

Category

Chemical class: Digitalis glycoside
Therapeutic class: Antiarrhythmic, cardiotonic

Pregnancy category: C

Indications

To treat heart failure, atrial flutter, atrial fibrillation, and paroxysmal atrial tachycardia with rapid digitalization ,
I.V.INJECTION
Adults.Loading: 10 to 15 mcg/kg in 3 divided doses every 6 to 8 hr, with first dose equal to 50% of total dose. Maintenance: 125 to 350 mcg daily once or twice daily. Children over age 10. Loading: 8 to 12 mcg/ kg in 3 or more divided doses, with first dose equal to 50% of total dose. Subsequent digoxin 319 D doses given every 6 to 8 hr. Maintenance: 2 to 3 mcg/kg once daily. Children ages 6 to 10. Loading: 15 to 30 mcg/kg in 3 or more divided doses, with first dose equal to 50% of total dose. Subsequent doses given every 6 to 8 hr. Maintenance: 4 to 8 mcg/kg daily in 2 divided doses. Children ages 2 to 5. Loading: 25 to 35 mcg/ kg in 3 or more divided doses, with first dose equal to 50% of total dose. Subsequent doses given every 6 to 8 hr. Maintenance: 6 to 9 mcg/kg daily in 2 divided doses. Infants ages 1 to 24 months. Loading: 30 to 50 mcg/kg in 3 or more divided doses, with first dose equal to 50% of total dose. Subsequent doses every 6 to 8 hr. Maintenance: 7.5 to 12 mcg/kg daily in 2 divided doses. Full-term neonates. Loading: 20 to 30 mcg/ kg in 3 or more divided doses, with first dose equal to 50% of total dose. Subsequent doses given every 6 to 8 hr. Maintenance: 5 to 8 mcg/kg daily in 2 divided doses. Premature neonates.Loading: 15 to 25 mcg/kg in 3 or more divided doses, with first dose equal to 50% of total dose. Subsequent doses given every 6 to 8 hr. Maintenance: 4 to 6 mcg/kg daily in 2 divided doses. ELIXIR,
Adults. Loading: 10 to 15 mcg/kg total dose given in 3 divided doses every 6 to 8 hr, with first dose equal to 50% of total dose. Maintenance: 125 to 500 mcg daily. Children over age 10. Loading: 10 to 15 mcg/kg total given in 3 divided doses every 6 to 8 hr, with first dose equal to 50% of total dose. Maintenance: 2.5 to 5 mcg/kg daily. Children ages 5 to 10. Loading: 20 to 35 mcg/kg in 3 divided doses every 6 to 8 hr. Maintenance: 5 to 10 mcg/kg daily in 2 divided doses. Children ages 2 to 5.Loading: 30 to 40 mcg/ kg in 3 divided doses every 6 to 8 hr. Maintenance: 7.5 to 10 mcg/kg daily in 2 divided doses. Infants ages 1 to 24 months. Loading: 35 to 60 mcg/kg in 3 divided doses every 6 to 8 hr. Maintenance: 10 to 15 mcg/kg daily in 2 divided doses. Full-term neonates. Loading: 25 to 35 mcg/ kg in 3 divided doses every 6 to 8 hr. Maintenance: 6 to 10 mcg/kg daily in 2 divided doses. Premature neonates.Loading: 20 to 30 mcg/ kg in 3 divided doses every 6 to 8 hr. Maintenance: 5 to 7.5 mcg/kg daily in 2 divided doses.
DOSAGE ADJUSTMENT Dosage carefully adjusted for patients who are elderly or debilitated or have implanted pacemakers because toxicity may develop at doses tolerated by most patients. Route Onset Peak Duration P.O. 30–120 min 6–8 hr 3–4 days I.V. 5–30 min 1–5 hr 3–4 days

Mechanism of Action

Increases the force and velocity of myocardial contraction, resulting in positive inotropic effects. Digoxin produces antiarrhythmic effects by decreasing the conduction rate and increasing the effective refractory period of the AV node.

Contraindications

Hypersensitive carotid sinus syndrome, hypersensitivity to digoxin, presence or history of digitalis toxicity or idiosyncratic reaction to digoxin, ventricular fibrillation, ventricular tachycardia unless heart failure occurs unrelated to digoxin therapy

Interactions

adsorbent antidiarrheals, such as kaolin and pectin; bulk laxatives; cholestyramine; colestipol; oral neomycin; sulfasalazine: Inhibited digoxin absorption amiodarone, propafenone: Elevated blood digoxin level, possibly to toxic level antacids: Inhibited digoxin absorption antiarrhythmics, pancuronium, parenteral calcium salts, rauwolfia alkaloids, sympathomimetics: Increased risk of arrhythmias diltiazem, verapamil: Increased blood digoxin level, possibly excessive bradycardia edrophonium: Excessive slowing of heart rate erythromycin, neomycin, tetracycline: Possibly increased blood digoxin level hypokalemia-causing , potassium-wasting diuretics: Increased risk of digitalis toxicity from hypokalemia indomethacin: Decreased renal clearance digoxin 320 and increased blood level of digoxin magnesium sulfate (parenteral): Possibly cardiac conduction changes and heart block quinidine, quinine: Increased blood digoxin level spironolactone: Increased half-life and risk of adverse effects of digoxin succinylcholine: Increased risk of digoxininduced arrhythmias sucralfate: Decreased digoxin absorption high-fiber food: Inhibited digoxin absorption

Side Efect

CNS: Confusion, depression, drowsiness, extreme weakness, headache, syncope
CV: Arrhythmias, heart block
EENT: Blurred vision, colored halos around objects
GI: Abdominal discomfort or pain, anorexia, diarrhea, nausea, vomiting
Other: Electrolyte imbalances

Cautions

Give parenteral digoxin undiluted, or dilute with a fourfold or greater volume of sterile water for injection, normal saline solution, or D5W for I.V. administration. Once diluted, give immediately. Discard if solution is markedly discolored or contains precipitate.

Before giving each dose, take patient’s apical pulse and notify prescriber if it’s below 60 beats/minute (or other specified level).

Monitor patient closely for signs of digitalis toxicity, such as altered mental status, arrhythmias, heart block, nausea, vision disturbances, and vomiting. If they appear, notify prescriber, check serum digoxin level as ordered, and expect to withhold drug until level is known. Monitor ECG tracing continuously.

If patient has acute or unstable chronic atrial fibrillation, assess for drug effectiveness.Ventricular rate may not normalize even when serum drug level falls within therapeutic range; raising the dosage probably won’t produce a therapeutic effect and may lead to toxicity.

Frequently obtain ECG tracings as ordered in elderly patients because of their smaller body mass and reduced renal clearance. Elderly patients, especially those with coronary insufficiency, are more susceptible to arrhythmias—particularly ventricular fibrillation—if digitalis toxicity occurs.

Monitor paptient’s serum potassium level regularly because hypokalemia predisposes to digitalis toxicity and serious arrhythmias. Also monitor potassium level often when giving potassium salts because hyperkalemia in patients receiving digoxin can be fatal.

PATIENT SAFTY

Stress importance of taking digoxin exactly as prescribed. Warn about possible toxicity from taking too much and decreased effectiveness from taking too little.

Instruct patient to take digoxin at same time each day to help increase compliance.

Teach patient how to take her pulse, and instruct her to do so before each dose. Urge her to notify prescriber if pulse falls below 60 beats/minute or suddenly increases.

Inform patient that small, white 0.25-mg tablets can easily be confused with other . Caution against carrying digoxin in anything other than its original labeled container.

Emphasize need to use special dropper supplied with elixir to ensure accurate dose measurement.

Instruct patient to take a missed dose as soon as she remembers if within 12 hours of scheduled dose. If not, urge her to notify prescriber immediately.

Urge patient to notify prescriber if she experiences

Side Efect

, such as GI distress or pulse changes.

Instruct patient to carry medical identification that indicates her need for digoxin.

Advise patient to consult prescriber before using other , including OTC products.

Category

Chemical class: Digoxin-specific antigenbinding fragments
Therapeutic class: Digitalis glycoside antidote

Pregnancy category: C

digoxin immune Fab (ovine) 321 D

Indications

To treat acute toxicity from a known amount of digoxin elixir or tablets
I.V.INJECTION Adults and children.Individualized dosage based on amount ingested. Dose (mg) 5 dose ingested (mg) multiplied by 0.8 and then divided by 0.5, multiplied by 38, and rounded up to next whole vial. To treat acute toxicity from a known amount of digoxin capsules, digitoxin tablets, or I.V. injection of digoxin or digitoxin
I.V.INJECTION Adults and children.Individualized dosage based on amount ingested. Dose (mg) 5 dose ingested (mg) divided by 0.5, then multiplied by 38 and rounded up to next whole vial. To treat acute toxicity from an unknown amount of digoxin or digitoxin during long-term therapy
I.V.INJECTION Adults and children.Individualized dosage for digoxin toxicity: dose (mg) 5 serum digoxin level (ng/ml) multiplied by body weight (kg), then divided by 100, and then multiplied by 38. Individualized dosage for digitoxin toxicity: dose (mg) 5 serum digitoxin level (ng/ml) multiplied by body weight (kg) and then divided by 1,000, multiplied by 38, and rounded up to next whole vial.
DOSAGE ADJUSTMENT Higher dose administered, as prescribed, if the dose based on ingested amount differs substantially from the dose based on serum digoxin or digitoxin level. Dose repeated after several hours, if needed. Route Onset Peak Duration I.V. 15–30 min Unknown 8–12 hr

Mechanism of Action

Binds with digoxin or digitoxin molecules. The resulting complex is excreted through the kidneys. As the free serum digoxin level declines, tissue-bound digoxin enters the serum and also is bound and excreted.

Contraindications

Hypersensitivity to digoxin immune Fab

Side Efect

CV: Increased ventricular rate (in atrial fibrillation), worsening of heart failure or low cardiac output
Other: Allergic reaction (difficulty breathing, urticaria), febrile reaction, hypokalemia

Cautions

Expect each 38-mg vial of purified digoxin immune Fab to bind about 0.5 mg of digoxin or digitoxin.

To reconstitute for I.V. use, dissolve 38 mg in 4 ml of sterile water for injection to yield 9.5 mg/ml. Mix gently. Further dilute with normal saline solution to proper volume for I.V. infusion. For very small doses, reconstituted 38-mg vial may be diluted with 34 ml of normal saline solution to yield 1 mg/ml.
WARNING Before giving digoxin immune Fab to high-risk patient, test for allergic reaction as prescribed by diluting 0.1 ml of reconstituted drug in 9.9 ml sodium chloride for injection and then injecting 0.1 ml (9.5 mcg/0.1 ml) intradermally. After 20 minutes, observe for an urticarial wheal surrounded by erythema. Alternatively, perform a scratch test by placing one drop of 9.5 mcg/0.1 ml dilution on patient’s skin and making a 1/40 scratch through the drop with a sterile needle. Inspect site in 20 minutes. Test is considered positive if it produces a wheal surrounded by erythema. If test causes a systemic reaction, apply tourniquet above test site, notify prescriber, and prepare to respond to anaphylaxis. Be aware that if a skin or systemic reaction occurs, additional drug shouldn’t be given unless essential; if more of the drug must be given, expect prescriber to pretreat patient with corticosteroids and diphenhydramine. Prescriber should be on standby to treat anaphylaxis.

For an infant, reconstitute digoxin immune Fab as ordered and administer with a tuberculin syringe.

When administering to a child, watch for fluid volume overload.

When giving a large dose, expect a faster onset but watch closely for febrile reaction.

Give I.V. infusion through a 0.22-micron membrane filter over 30 minutes. Keep in mind that drug may be given by rapid I.V. injection if cardiac arrest is imminent.

Monitor serum potassium level often, especially during first few hours of theradigoxin immune Fab (ovine) 322 py. Potassium level may drop rapidly.

PATIENT SAFTY

Inform patient of the purpose of digoxin immune Fab and how it will be given.

Advise patient to notify you immediately if she experiences

Side Efect

, especially difficulty breathing and urticaria.

Category

Chemical class: Semisynthetic ergot alkaloid
Therapeutic class: Antimigraine

Pregnancy category: X

Indications

To treat acute migraine with or without aura I.V. INJECTION
Adults. 1 mg, repeated in 1 hr, if needed. Maximum: 6 mg/wk.

IM

Adults. 1 mg at first sign of headache, repeated every hr up to 3 mg, if needed. Maximum: 3 mg/24 hr, 6 mg/wk.
NASAL SPRAY
Adults. 1 spray (0.5 mg) in each nostril, repeated in 15 min for a total dose of 2 sprays in each nostril or 2 mg. Maximum: 3 mg/24 hr, 4 mg/wk. Route Onset Peak Duration I.V. In 5 min 15 min– About 8 hr 2 hr I.M. 15–30 min 15 min– 3–4 hr 2 hr Nasal In 30 min 30–60 min Unknown

Mechanism of Action

Produces intracranial and peripheral vasoconstriction by binding to all known 5hydroxytryptamine1(5-HT1) receptors, alpha1and alpha2-adrenergic receptors, and dopaminergic receptors. Activation of 5-HT1receptors on intracranial blood vessels probably constricts large intracranial arteries and closes arteriovenous anastomoses to relieve migraine headache. Activation of 5-HT1receptors on sensory nerves in the trigeminal system also may inhibit the release of pro-inflammatory neuropeptides. Peripherally, dihydroergotamine causes vasoconstriction by stimulating alphaadrenergic receptors. At therapeutic doses, it inhibits norepinephrine reuptake, increasing vasoconstriction. Drug constricts veins more than arteries, increasing venous return while decreasing venous stasis and pooling.

Contraindications

Coronary artery disease, including vasospasm; hemiplegic or basilar migraine; hypersensitivity to dihydroergotamine or other ergot alkaloids; malnutrition; peripheral vascular disease or after vascular surgery; pregnancy; sepsis; severe hepatic or renal impairment; severe pruritus; uncontrolled hypertension; use of macrolide antibiotics or protease inhibitors; use within 24 hours of 5-HT1agonist, ergotamine-containing or ergot-type drug, or methysergide

Interactions

beta blockers: Possibly peripheral vasoconstriction and peripheral ischemia, increased risk of gangrene macrolides, protease inhibitors: Possibly increased risk of vasospasm, acute ergotism with peripheral ischemia nitrates: Decreased antianginal effects of nitrates other ergot , including ergoloid mesylates, ergonovine, methylergonovine, methysergide, and sumatriptan: Increased risk of serious adverse effects from nasal dihydroergotamine systemic vasoconstrictors: Risk of severe hypertension smoking: Possibly increased ischemic response to ergot therapy

Side Efect

CNS: Anxiety, confusion, dizziness, fatigue, headache, paresthesia, somnolence, weakness
CV: Bradycardia, chest pain, peripheral vasospasm (calf or heel pain with exertion, cool and cyanotic hands and feet, leg weakness, weak or absent pulses), tachycardia
EENT: Abnormal vision; dry mouth; episdihydroergotamine mesylate 323 D taxis, nasal congestion or rhinitis, and sore nose (
NASAL SPRAY); miosis; pharyngitis; sinusitis; taste perversion
GI: Diarrhea, nausea, vomiting
MS: Muscle stiffness
SKIN: Localized edema of face, feet, fingers, and lower legs; sensation of heat or warmth; sudden diaphoresis

Cautions

WARNING Monitor patient for signs of dihydroergotamine overdose, such as abdominal pain, confusion, delirium, dizziness, dyspnea, headache, nausea, pain in legs or arms, paresthesia, seizures, and vomiting.

Assess patient’s peripheral pulses, skin sensation, warmth, and capillary refill. After giving nasal dihydroergotamine, monitor patient for signs of widespread blood vessel constriction and

Side Efect

caused by decreased circulation to many body areas.

PATIENT SAFTY

Instruct patient to use
NASAL SPRAY when headache pain—not aura—begins.

Teach her to prime spray pump by squeezing it four times.

Advise patient to wait 15 minutes between each set of
NASAL SPRAYs.

Encourage patient to lie down in a quiet, dark room after using drug.

Instruct patient to use more dihydroergotamine if headache returns or worsens but not to exceed maximum prescribed amount or frequency.

Remind patient to take drug only as needed, not on a daily basis.

Instruct patient to discard residual nasal spray in an open ampule after 8 hours.

If patient has a headache different from her usual migraines, caution her not to use dihydroergotamine and to notify prescriber.

Inform patient that nasal drug won’t relieve pain other than throbbing headaches.

Advise patient to avoid alcohol, which can cause or worsen headaches, and to avoid smoking, which may cause an ischemic response.

Warn patient about possible dizziness during or after a migraine for which she took dihydroergotamine.

Category

Chemical class: Sterol derivative, vitamin D analogue
Therapeutic class: Antihypocalcemic, antihypoparathyroid

Pregnancy category: C

Indications

To treat hypocalcemic and idiopathic tetany ,, Adults and adolescents. Initial: 0.75 to 2.5 mg daily for 3 days for acute cases; 0.25 to 0.5 mg daily for 3 days for less acute cases. Maintenance: 0.25 mg/wk to 1 mg daily, as needed to maintain normal serum calcium level. To treat hypoparathyroidism ,, Adults and adolescents. Initial: 0.75 to 2.5 mg daily for several days. Maintenance: 0.2 to 1 mg daily. Children.Initial: 1 to 5 mg daily for 4 days; then continued or decreased to one-quarter the dose. Maintenance: 0.5 to 1.5 mg daily. Route Onset Peak Duration P.O. Several hr Unknown Up to 9 wk

Mechanism of Action

Stimulates intestinal calcium absorption and mobilizes bone calcium when parathyroid hormone and renal tissue fail to raise the serum calcium level.

Contraindications

Hypercalcemia, hypersensitivity to vitamin D, hypervitaminosis D, malabsorption syndrome, renal dysfunction

Interactions

aluminum-containing antacids: Possibly increased serum aluminum level, leading to toxicity barbiturates,
phenytoin: Decreased half-life and therapeutic effects of vitamin D calcium-containing , thiazide diuretics: Risk of hypercalcemia in patients with hypoparathyroidism cholestyramine, colestipol, mineral oil: dihydrotachysterol 324 Decreased vitamin D absorption digitalis glycosides: Possibly hypercalcemia; possibly potentiated effects of digitalis glycosides, resulting in arrhythmias magnesium-containing antacids: Risk of hypermagnesemia, especially in patients with chronic renal failure phosphorus-containing : Increased risk of hyperphosphatemia vitamin D analogues: Increased risk of vitamin D toxicity

Side Efect

Other: Vitamin D toxicity (long-term, high-dose therapy)

Cautions

After thyroid surgery, expect to give 0.25 mg once daily with 6 g of oral calcium lactate until danger of tetany has passed.

Monitor serum calcium level regularly to determine dosage schedule and detect or prevent hypercalcemia. The difference between therapeutic and toxic doses may be small.

Watch closely for signs of vitamin D toxicity: abdominal cramps, amnesia, anorexia, ataxia, coma, constipation, depression, diarrhea, disorientation, hallucinations, headache, hypotonia, lethargy, nausea, syncope, tinnitus, vertigo, vomiting, and weakness. Renal impairment may cause albuminuria, polydipsia, and polyuria. Delayed treatment can result in death from cardiac and renal failure caused by widespread calcification of soft tissues, including the heart, blood vessels, kidneys, and lungs.

If toxicity occurs, notify prescriber and expect to stop dihydrotachysterol immediately. Place patient on bed rest, administer fluids and a laxative, and give low-calcium diet as ordered. For hypercalcemic crisis with dehydration, prepare to give I.V. normal saline solution and a loop diuretic (such as furosemide or ethacrynic acid) to increase urinary calcium excretion.

PATIENT SAFTY

Stress importance of not exceeding prescribed dihydrotachysterol dosage because of the risk of vitamin D toxicity.

If patient detects signs of toxicity, caution her not to take the next dose and to notify prescriber immediately.

Advise patient to drop solution directly into her mouth or to mix it with fruit juice, cereal, or other food.

Tell patient to take a missed dose as soon as she remembers unless it’s nearly time for next dose. Warn her not to double it.

Advise patient to avoid OTC and dietary supplements that contain aluminum, calcium, phosphorus, or vitamin D, unless directed by prescriber. Also advise her to avoid antacids that contain magnesium.

Urge patient to keep follow-up appointments and to have her serum calcium level measured periodically.

Category

Chemical class: Benzothiazepine derivative
Therapeutic class: Antianginal, antiarrhythmic, antihypertensive

Pregnancy category: C

Indications

To treat Prinzmetal’s (variant) angina and chronic stable angina Adults and adolescents. Initial: 30 mg t.i.d. or q.i.d. before meals and at bedtime, increased every 1 or 2 days as appropriate. Maximum: 360 mg daily in divided doses t.i.d. or q.i.d. Adults and adolescents.Initial: 180 mg daily, increased every 7 to 14 days as needed. Maximum: 360 mg daily. To control hypertension Adults and adolescents.Initial: 180 to 240 mg daily, adjusted after 14 days as appropriate. Maximum: 360 mg daily. S.R. Adults and adolescents.Initial: 60 to 120 mg b.i.d., adjusted after 14 days as appropriate. Maximum: 360 mg daily. diltiazem hydrochloride 325 D Adults and adolescents. Initial: 30 mg t.i.d. or q.i.d. before meals and at bedtime, increased every 1 or 2 days as appropriate. Maximum: 360 mg daily in divided doses t.i.d. or q.i.d.
Adults. Initial: 180 to 240 mg daily, adjusted after 14 days, as needed. Maximum: 540 mg daily. To treat atrial fibrillation, atrial flutter, and paroxysmal supraventricular tachycardia

IV

OR INJECTION Adults and adolescents.0.25 mg/kg given by bolus over 2 min. If response is inadequate after 15 min, 0.35 mg/kg given by bolus over 2 min. Then 10 mg/hr for continued reduction of heart rate after bolus, increased by 5 mg/hr, as needed. Maximum: 15 mg/hr for up to 24 hr. Route Onset Peak Duration P.O. 30–60 min In 2 wk Unknown P.O. () 2–3 hr In 2 wk Unknown P.O. (S.R.) Unknown In 2 wk Unknown I.V. In 3 min 2– 7 min 30 min– 10 hr*

Incompatibilities

Don’t give diltiazem through same I.V. line as acetazolamide, acyclovir, aminophylline, ampicillin sodium/sulbactam sodium, cefamandole, cefoperazone, diazepam, furosemide, heparin, hydrocortisone sodium succinate, methylprednisolone sodium succinate, mezlocillin, nafcillin, phenytoin, rifampin, or sodium bicarbonate.

Contraindications

Acute MI; cardiogenic shock; LownGanong-Levine or Wolff-Parkinson-White syndrome, secondor third-degree AV block, and sick sinus syndrome, unless artificial pacemaker is in place; pulmonary edema; systolic blood pressure below 90 mm Hg; ventricular tachycardia (wide complex)

Interactions

anesthetic: Additive hypotension; possibly decreased cardiac contractility, conductivity, and automaticity benzodiazepines: Increased risk of prolonged sedation
beta blockers: Possibly increased risk of adverse cardiovascular effects buspirone: Increased effects and risk of buspirone toxicity carbamazepine, cyclosporine, lovastatin, quinidine, theophyllines: Decreased hepatic clearance and increased serum levels of these , leading to toxicity
cimetidine: Decreased diltiazem metabolism, increased blood diltiazem level digoxin: Increased blood digoxin level lithium: Possibly neurotoxicity diltiazem hydrochloride 326 *For infusion; 1 to 3 hr for injection. Ca++ Ca++ Ca++ Ca++ Cell exterior Cell interior Cell membrane Calcium channel Calcium movement blocked by diltiazem

Mechanism of Action

Diltiazem inhibits calcium movement into coronary and vascular smooth-muscle cells by blocking slow calcium channels in cell membranes, as shown. This action decreases intracellular calcium, which:

inhibits smooth-muscle cell contractions

decreases myocardial oxygen demand by relaxing coronary and vascular smooth muscle, reducing peripheral vascular resistance and systolic and diastolic blood pressures

slows AV conduction time and prolongs AV nodal refractoriness

interrupts the reentry circuit in AV nodal reentrant tachycardias.
NSAIDs: Possibly antagonized antihypertensive effect of diltiazem prazocin: Possibly increased risk of hypotension procainamide: Possibly increased risk of prolonged QT interval
quinidine: Increased risk of adverse quinidine effects
rifampin: Decreased blood diltiazem level to undetectable amounts

Side Efect

CNS: Abnormal gait, amnesia, asthenia, depression, dizziness, dream disturbances, extrapyramidal reactions, fatigue, hallucinations, headache, insomnia, nervousness, paresthesia, personality change, somnolence, syncope, tremor, weakness
CV: Angina, atrial flutter, AV block (first-, second-, and third-degree), bradycardia, bundle-branch block, heart failure, hypotension, palpitations, peripheral edema, PVCs, sinus arrest, sinus tachycardia, 12-lead ECG abnormalities, ventricular fibrillation, ventricular tachycardia
EENT: Amblyopia, dry mouth, epistaxis, eye irritation, gingival bleeding and hyperplasia, gingivitis, nasal congestion, retinopathy, taste perversion, tinnitus
ENDO: Hyperglycemia
GI: Anorexia, constipation, diarrhea, elevated liver function test results, indigestion, nausea, thirst, vomiting
GU: Acute renal failure, impotence, nocturia, polyuria, sexual dysfunction
HEME: Hemolytic anemia, leukopenia, prolonged bleeding time, thrombocytopenia
MS: Arthralgia, muscle spasms, myalgia
RESP: Cough, dyspnea
SKIN: Alopecia, diaphoresis, erythema multiforme, exfoliative dermatitis, flushing, leukocytoclastic vasculitis, petechiae, photosensitivity, pruritus, purpura, rash, StevensJohnson syndrome, toxic epidermal necrolysis, urticaria
Other: Angioedema, hyperuricemia, weight gain

Cautions

Use diltiazem cautiously in patients with impaired hepatic or renal function, and monitor liver and renal function, as appropriate; drug is metabolized mainly in the liver and excreted by the kidneys.
WARNING Monitor patient’s blood pressure, pulse rate, and heart rate and rhythm by continuous ECG as appropriate during therapy. Keep emergency equipment and available.

Assess patient for signs and symptoms of heart failure.

If patient takes digoxin, watch for digitalis toxicity (nausea, vomiting, halo vision, elevated serum digoxin level).

Administer sublingual nitroglycerin, as prescribed, during diltiazem therapy.

Expect to discontinue drug if adverse skin reactions, usually transient, persist.

PATIENT SAFTY

Explain that regular tablets can be crushed but that capsules and tablets must be swallowed whole.
WARNING Tell patient that stopping drug suddenly may have life-threatening effects.

Advise patient to monitor blood pressure and pulse rate regularly and to report significant changes to prescriber.

Urge patient to report chest pain, difficulty breathing, dizziness, fainting, irregular heartbeat, rash, or swollen ankles.

Instruct patient to maintain good oral hygiene, perform gum massage, and see a dentist every 6 months to prevent gingival bleeding and hyperplasia and gingivitis.

Category

Chemical class: Ethanolamine derivative
Therapeutic class: Antiemetic, antivertigo

Pregnancy category: B

Indications

To treat nausea, vomiting, dizziness, or vertigo associated with motion sickness CHEWABLE ,, SYRUP, Adults and adolescents. 50 to 100 mg every 4 to 6 hr, p.r.n. Maximum: 400 mg/24 hr. Children ages 6 to 12. 25 to 50 mg every 6 to 8 hr, p.r.n. Maximum: 150 mg/24 hr. Children ages 2 to 6. 12.5 to 25 mg every 6 to 8 hr, p.r.n. Maximum: 75 mg/24 hr.
I.M.INJECTION Adults and adolescents.50 mg every 4 hr, p.r.n. dimenhydrinate 327 D Children.1.25 mg/kg or 37.5 mg/m2every 6 hr, p.r.n. Maximum: 300 mg daily.
IV: OR INJECTION Adults and adolescents. 50 mg in 10 ml of normal saline solution administered slowly, over at least 2 min, every 4 hr, p.r.n. Children.1.25 mg/kg or 37.5 mg/m2in 10 ml of normal saline solution administered slowly, over at least 2 min, every 6 hr, p.r.n. Maximum: 300 mg daily. Route Onset Peak Duration P.O. Unknown Unknown 3–6 hr I.M. 20–30 min Unknown 3–6 hr I.V. Immediate Unknown 3–6 hr

Mechanism of Action

May inhibit vestibular stimulation and labyrinthine stimulation and function by acting on the otolith system and, with larger doses, on the semicircular canals.

Contraindications

Age less than 1 month, hypersensitivity to dimenhydrinate or its components

Interactions

aminoglycosides, other ototoxic : Masked symptoms of ototoxicity anticholinergics, with anticholinergic activity: Potentiated anticholinergic effects of dimenhydrinate apomorphine: Possibly decreased emetic response to apomorphine in treatment of poisoning barbiturates, other
CNS depressants: Possibly increased CNS depression
MAO inhibitors: Increased anticholinergic and CNS depressant effects of dimenhydrinate
alcohol use: Possibly increased CNS depression

Side Efect

CNS: Confusion, drowsiness, hallucinations, nervousness, paradoxical stimulation
CV: Hypotension, palpitations, tachycardia
EENT: Blurred vision, diplopia, dry eyes, dry mouth, nasal congestion
GI: Anorexia, constipation, diarrhea, epigastric discomfort, nausea, vomiting
GU: Dysuria
HEME: Hemolytic anemia
RESP: Thickening of bronchial secretions, wheezing
SKIN: Photosensitivity, rash, urticaria
Other: Anaphylaxis

Cautions

WARNING Be aware that I.V. dimenhydrinate shouldn't be administered to premature or full-term neonates. Some I.V. preparations may contain benzyl alcohol, which can cause a fatal toxic syndrome characterized by CNS, respiratory, circulatory, and renal impairment and metabolic acidosis.
WARNING Be aware that the 50-mg/ml concentration of dimenhydrinate is intended for I.M. use. For I.V. use, the solution must be diluted further with at least 10 ml of diluent, such as D5W or normal saline solution, for each milliliter of dimenhydrinate.

Monitor patients with prostatic hyperplasia, stenosing peptic ulcer, pyloroduodenal obstruction, bladder neck obstruction, angle-closure glaucoma, bronchial asthma, or cardiac arrhythmias for worsening of these conditions caused by anticholinergic effects.

Monitor elderly patients for increased sensitivity to dimenhydrinate, such as excessive drowsiness, confusion, and restlessness.

Assess patients, especially children and elderly patients, for evidence of paradoxical stimulation, such as nightmares, unusual excitement, nervousness, restlessness, or irritability.

Store parenteral drug at 15° to 30° C (59° to 86° F); don’t freeze.

PATIENT SAFTY

Because dimenhydrinate may cause drowsiness, instruct patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to inform health care providers about dimenhydrinate therapy, especially if she’s being evaluated for medical conditions that are affected by this drug, such as appendicitis.

Instruct patient to avoid alcohol, sedatives, and tranquilizers while taking dimenhydrinate.

Encourage patient to use sunscreen to prevent photosensitivity reactions.

Category

Chemical class: Ethanolamine derivative
Therapeutic class: Antianaphylactic adjunct, antidyskinetic, antiemetic, antihistamine, antitussive (syrup), antivertigo, sedativehypnotic

Pregnancy category: B

Indications

To treat hypersensitivity reactions, such as perennial and seasonal allergic rhinitis, vasomotor rhinitis, allergic conjunctivitis, uncomplicated allergic skin eruptions, and transfusion reactions , Adults and adolescents. 25 to 50 mg every 4 to 6 hr, p.r.n. Maximum: 300 mg daily. Children ages 6 to 12. 12.5 to 25 mg every 4 to 6 hr. Maximum: 150 mg daily. Children up to age 6. 6.25 to 12.5 mg every 4 to 6 hr. ELIXIR Adults and adolescents. 25 to 50 mg every 4 to 6 hr, p.r.n. Maximum: 300 mg daily. Children.1.25 mg/kg every 4 to 6 hr. Maximum: 300 mg daily. I.V.OR
I.M.INJECTION Adults and adolescents.10 to 50 mg every 4 to 6 hr up to 100 mg/dose, if needed. Maximum: 400 mg daily. Children.1.25 mg/kg every 4 to 6 hr. Maximum: 300 mg daily. To treat sleep disorders , Adults and adolescents. 50 mg 20 to 30 min before bedtime. To provide antitussive effects ELIXIR Adults and adolescents.25 mg every 4 hr. Maximum: 100 mg/24 hr. Children ages 6 to 12. 12.5 mg every 4 to 6 hr. Maximum: 75 mg daily. Children ages 2 to 6. 6.25 mg every 4 to 6 hr. Maximum: 25 mg daily. To prevent motion sickness or treat vertigo , ELIXIR, Adults and adolescents. 25 to 50 mg every 4 to 6 hr, p.r.n. Maximum: 300 mg daily. Children.1 to 1.5 mg/kg every 4 to 6 hr, p.r.n. Maximum: 300 mg daily. I.V.OR
I.M.INJECTION Adults and adolescents.Initial: 10 mg. Increased to 20 to 50 mg every 2 to 3 hr, if needed. Maximum: 100 mg/dose, 400 mg daily. Children.1 to 1.5 mg/kg I.M. every 4 to 6 hr, p.r.n. Maximum: 300 mg daily. To treat symptoms of Parkinson’s disease and drug-induced extrapyramidal reactions in elderly patients who can’t tolerate more potent antidyskinetic , ELIXIR,
Adults.25 mg t.i.d. increased gradually to 50 mg q.i.d., if needed. Maximum: 300 mg daily. I.V.OR
I.M.INJECTION Adults and adolescents.10 to 50 mg q.i.d., as needed. Maximum: 100 mg/dose, 400 mg daily. Route Onset Peak Duration P.O. 15–60 min 1–3 hr 6–8 hr I.V. Immediate 1–3 hr 6–8 hr I.M. 30 min 1–3 hr 6–8 hr

Mechanism of Action

Binds to central and peripheral H1receptors, competing with histamine for these sites and preventing it from reaching its site of action. By blocking histamine, diphenhydramine produces antihistamine effects, inhibiting respiratory, vascular, and GI smooth-muscle contraction; decreasing capillary permeability, which reduces wheals, flares, and itching; and decreasing salivary and lacrimal gland secretions. Diphenhydramine produces antidyskinetic effects, possibly by inhibiting acetylcholine in the CNS. It also produces antitussive effects by directly suppressing the cough center in the medulla oblongata in the brain. Diphenhydramine’s antiemetic and antivertigo effects may be related to its ability to bind to CNS muscarinic receptors and depress vestibular stimulation and labyrinthine function. Its sedative effects are related to its CNS depressant action. diphenhydramine hydrochloride 329 D

Contraindications

Bladder neck obstruction, hypersensitivity to diphenhydramine or its components, lower respiratory tract symptoms (including asthma), MAO inhibitor therapy, narrow-angle glaucoma, pyloroduodenal obstruction, stenosing peptic ulcer, symptomatic benign prostatic hyperplasia

Interactions

apomorphine: Possibly decreased emetic response in treatment of poisoning barbiturates, other
CNS depressants: Possibly increased CNS depression
MAO inhibitors: Increased anticholinergic and CNS depressant effects of diphenhydramine
alcohol use: Possibly increased CNS depression

Side Efect

CNS: Confusion, dizziness, drowsiness
CV: Arrhythmias, palpitations, tachycardia
EENT: Blurred vision, diplopia
GI: Epigastric distress, nausea
HEME: Agranulocytosis, hemolytic anemia, thrombocytopenia
RESP: Thickened bronchial secretions
SKIN: Photosensitivity

Cautions

Expect to give parenteral form of diphenhydramine only when oral ingestion isn’t possible.

Keep elixir container tightly closed. Protect elixir and parenteral forms from light.

Expect to discontinue drug at least 72 hours before skin tests for allergies because drug may inhibit cutaneous histamine response, thus producing false-negative results.

PATIENT SAFTY

Instruct patient to take diphenhydramine at least 30 minutes before exposure to situations that may cause motion sickness.

Advise her to take drug with food to minimize GI distress.

Urge patient to avoid alcohol while taking diphenhydramine.

Instruct her to use sunscreen to prevent photosensitivity reactions.

Advise patient to avoid taking other OTC that contain diphenhydramine to prevent additive effects.

Category

Chemical class: Pyrimidine
Therapeutic class: Coronary vasodilator, diagnostic aid, platelet aggregation inhibitor

Pregnancy category: B

Indications

To prevent thromboembolic complications of cardiac valve replacement
Adults.75 to 100 mg q.i.d. with coumarin or indanedione derivative anticoagulant. To aid diagnosis during thallium perfusion imaging of myocardium
IV:
Adults. 0.57 mg/kg in 50 ml of D5W infused over 4 min. Maximum: 60 mg. Route Onset Peak Duration I.V. Unknown 3.8– Unknown 8.7 min*

Mechanism of Action

May increase the intraplatelet level of adenosine, which causes coronary vasodilation and inhibits platelet aggregation. Dipyridamole also may increase the intraplatelet level of cyclic adenosine monophosphate (cAMP) and may inhibit formation of the potent platelet activator stimulant thromboxane A2, which decreases platelet activation.Vasodilation and increased blood flow occur preferentially in nondiseased coronary vessels, which results in redistribution of blood away from significantly diseased vessels. These changes in perfusion are observed during thallium imaging studies.

Contraindications

Asthma (I.V.), hypersensitivity to dipyridamole or its components, hypotension, unstable angina pectoris dipyridamole 330 * After start of infusion, for increased velocity of coronary artery blood flow.

Interactions

adenosine: Potentiated effects of adenosine cefamandole, cefoperazone, cefotetan, plicamycin,
valproic acid: Possibly hypoprothrombinemia and increased risk of bleeding heparin, NSAIDs, thrombolytics: Possibly increased risk of bleeding
theophylline: Reversal of coronary vasodilation caused by dipyridamole, possibly falsenegative thallium imaging result

Side Efect

CNS: Dizziness, headache
CV: Angina, arrhythmias, ECG changes (specifically, ST-segment and T-wave changes)
GI: Abdominal pain, diarrhea, nausea, vomiting
RESP: Dyspnea
SKIN: Flushing, pruritus, rash

Cautions

Protect I.V. form of dipyridamole from direct light and freezing.

Monitor blood pressure, pulse rate and rhythm, and breath sounds every 10 to 15 minutes during I.V. infusion.

Keep parenteral aminophylline available to relieve

Side Efect

to dipyridamole infusion.

At therapeutic doses, expect adverse reactions to be minimal and transient. They typically resolve with long-term use.

PATIENT SAFTY

Urge patient to take dipyrinamole at least 1 hour before or 2 hours after meals for faster absorption. If she experiences GI distress, advise her to take drug with meals or milk.

Advise patient to take drug at evenly spaced intervals.

Inform patient that drug commonly is taken with other anticoagulants.

Urge her to keep appointments for coagulation tests.

Instruct patient to seek immediate emergency treatment if chest pain occurs.

Caution patient to consult prescriber before taking aspirin and other OTC NSAIDs because of the possible increased risk of bleeding.

Advise patient to notify all health care providers about dipyridamole use.

Category

Chemical: Semisynthetic macrolide Therapeutic: Antibiotic

Pregnancy category: C

Indications

To treat acute bacterial exacerbations and secondary bacterial infections in patients with bronchitis caused by Moraxella catarrhalis or Streptococcus pneumoniae, and uncomplicated skin and soft-tissue infections caused by methicillin-susceptible Staphylococcus aureus Adults and adolescents.500 mg daily for 7 days. To treat streptococcal pharyngitis Adults and adolescents.500 mg daily for 10 days. To treat community-acquired pneumonia caused by Legionella pneumophila, Mycoplasma pneumoniae, or S. pneumoniae Adults and adolescents.500 mg daily for 14 days.

Mechanism of Action

Binds with the 50S ribosomal subunit of the 70S ribosome in susceptible bacteria. This action inhibits RNA-dependent protein synthesis in bacterial cells, causing them to die.

Contraindications

Concurrent use of astemizole, cisapride, or pimozide; hypersensitivity to dirithromycin, erythromycin, other macrolide antibiotics, or their components; known, potential, or suspected bacteremia

Interactions

antacids, H2-receptor antagonists: Increased dirithromycin absorption astemizol, terfenadine: Possibly life-threatening arrhythmias
theophylline: Possibly increased serum theophylline level dirithromycin 331 D

Side Efect

CNS: Dizziness, headache, weakness
GI: Abdominal pain, diarrhea, nausea, pseudomembranous colitis, vomiting
SKIN: Pruritus, rash, urticaria

Cautions

Use dirithromycin cautiously in patients with impaired hepatic function. Monitor liver function test results as indicated because drug is metabolized in liver. PATIENTTEACHING

Instruct patient to take dirithromycin at the same time each day with food or within 1 hour of eating.

Caution patient not to cut, chew, or crush tablets.

Advise patient to store drug at room temperature in a dry place.

Instruct patient to complete the full course of prescribed therapy, even if she feels better before drug is gone.

Advise patient to notify prescriber immediately if GI problems persist.

Category

Chemical class: Substituted pyramide derivative
Therapeutic class: Class IA antiarrhythmic

Pregnancy category: C

Indications

To rapidly control ventricular arrhythmias
Adults. Loading: 300 mg (200 mg if patient weighs less than 50 kg [110 lb]). If no response within 6 hr, 200 mg given every 6 hr. If no response within 48 hr, drug discontinued or dosage carefully increased to 250 to 300 mg every 6 hr. To treat ventricular arrhythmias
Adults.400 to 800 mg daily in divided doses every 6 hr, limited to 400 mg daily if patient weighs less than 50 kg. Maximum: 800 mg daily. Children ages 12 to 18. 6 to 15 mg/kg daily in divided doses every 6 hr. Children ages 4 to 12. 10 to 15 mg/kg daily in divided doses every 6 hr. Children ages 1 to 4. 10 to 20 mg/kg daily in divided doses every 6 hr. Children under age 1. 10 to 30 mg/kg daily in divided doses every 6 hr.
DOSAGE ADJUSTMENT Initial dosage reduced to 100 mg every 6 to 8 hr for adults with cardiomyopathy or possible cardiac decompensation. In renal insufficiency, dosage reduced to 100 mg every 6 hr if creatinine clearance exceeds 40 ml/min/1.73 m2or hepatic function is impaired; to 100 mg every 8 hr if clearance is 30 to 40 ml/min/ 1.73 m2; to 100 mg every 12 hr if clearance is 15 to 29 ml/min/1.73 m2; and to 100 mg every 24 hr if clearance is less than 15 ml/ min/1.73 m2. ,
Adults.400 to 800 mg daily in divided doses every 12 hr, limited to 200 mg every 12 hr if patient weighs less than 50 kg. Maximum: 800 mg daily.

Mechanism of Action

Inhibits sodium influx through fast channels of myocardial cell membranes, thus increasing recovery period after repolarization. Disopyramide decreases automaticity in the His-Purkinje system and conduction velocity in atria, ventricles, and accessory pathways. It prolongs QRS and QT intervals in normal sinus rhythm and atrial arrhythmias. Drug has a potent negative inotropic effect. It also acts as an anticholinergic and increases peripheral vascular resistance.

Contraindications

Cardiogenic shock, congenital QT-interval prolongation, hypersensitivity to disopyramide or its components, secondor thirddegree AV block (without pacemaker), sick sinus syndrome

Interactions

antiarrhythmics: Widened QRS complex, prolonged QT interval, risk of arrhythmias, serious negative inotropic effects anticholinergics: Possibly additive antidisopyramide 332 cholinergic effects cisapride: Possibly increased risk of prolonged QT interval clarithromycin, erythromycin: Increased blood disopyramide level digoxin: Increased serum digoxin level hydantoins,
rifampin: Decreased blood disopyramide level insulin, oral antidiabetic : Possibly intensified antidiabetic effects
quinidine: Increased blood disopyramide level, decreased quinidine level, or both verapamil: Widened QRS complex, prolonged QT interval, possibly death

Side Efect

CNS: Depression, dizziness, fatigue, fever, headache, insomnia, nervousness, syncope
CV: Chest pain; conduction disturbances; edema; heart failure (new or worsened); hypercholesterolemia; hypertriglyceridemia; hypotension; palpitations; proarrhythmias, including torsades de pointes; ventricular fibrillation; ventricular tachycardia
EENT: Blurred vision; dry eyes, mouth, nose, and throat
ENDO: Gynecomastia, hypoglycemia
GI: Abdominal distention, anorexia, constipation, diarrhea, vomiting
GU: Impotence, urinary frequency and urgency, urine retention
HEME: Reversible agranulocytosis (rare), thrombocytopenia
MS: Muscle weakness
RESP: Dyspnea
SKIN: Decreased sweating, pruritus, rash, reversible cholestatic jaundice
Other: Hypokalemia, lupus erythematosus– like symptoms

Cautions

WARNING Because of disopyramide’s anticholinergic activity, avoid using drug in patients with glaucoma, myasthenia gravis, or urine retention.

Use disopyramide cautiousl,y and expect to reduce dosage in patients with impaired hepatic or renal function. Monitor hepatic and renal function, as ordered. Be aware that form shouldn’t be given to patients with severe renal insufficiency.

When changing from immediate-release to form, expect to start maintenance schedule 6 hours after last immediaterelease dose.

At therapeutic doses in hemodynamically uncompromised patients, expect drug to reduce cardiac output without decreasing resting sinus rate or affecting blood pressure. Keep in mind, however, that 2 mg/kg given I.V. over 3 minutes can increase heart rate and total peripheral resistance.

Monitor heart rate and rhythm by continuous ECG.

Assess serum electrolyte levels, especially potassium level, because drug may be ineffective in hypokalemia and its toxic effects enhanced in hyperkalemia.

If patient takes quinidine, expect to start disopyramide 6 to 12 hours after last dose of quinidine. If patient takes procainamide, expect to start disopyramide 3 to 6 hours after the last dose of procainamide. A loading dose may not be required in either case.

PATIENT SAFTY

Warn patient not to stop taking disopyramide abruptly; doing so may cause lifethreatening cardiac problems.

Advise patient to take a missed dose as soon as possible after she remembers, unless it’s nearly time for the next dose. Caution her against doubling the dose. Urge her to notify prescriber if she misses more than one dose.

Instruct patient to store drug at room temperature in a dry place.

Instruct patient to check her pulse rate regularly and report significant changes.

Urge patient to report blurred vision, constipation, difficulty urinating, dizziness, dry mouth, and trouble breathing.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to rise slowly from a lying or sitting position to reduce dizziness.

Urge patient to avoid becoming overheated during hot weather or exercise because of risk of heatstroke.

Category

Chemical class: Thiuram derivative
Therapeutic class: Alcohol abuse deterrent

Pregnancy category: Not rated

disulfiram 333 D

Indications

As adjunct to maintain sobriety in treatment of chronic alcoholism
Adults. Initial: Up to 500 mg daily for 1 to 2 wk. Maintenance: 125 to 500 mg daily. Maximum: 500 mg daily. Route Onset Peak Duration P.O. 1–2 hr Unknown Up to 14 days

Mechanism of Action

Interferes with the enzyme responsible for hepatic oxidation of acetaldehyde to acetate, which occurs during alcohol catabolism. Ingestion of even a small amount of alcohol after taking disulfiram raises the blood acetaldehyde level to 5 to 10 times normal. Disulfiram doesn’t alter the rate of alcohol elimination. Its major metabolite, diethyldithiocarbamate, inhibits norepinephrine synthesis and may be responsible for the drug’s hypotensive effect.

Contraindications

Alcohol intoxication; coronary artery occlusion; hypersensitivity to disulfiram, its components, rubber, pesticides, or fungicides; psychosis; recent use of alcohol, alcoholcontaining preparations, metronidazole, or paraldehyde; severe myocardial disease

Interactions

alfentanil: Decreased plasma clearance and prolonged duration of action of alfentanil amoxicillin-clavulanate, bacampicillin: Possibly disulfiram-alcohol reaction ascorbic acid: Possibly interference with disulfiram-alcohol reaction
CNS depressants: Possibly increased CNS depressant effects of either drug isoniazid: Increased risk of additive neurotoxic effect of disulfiram; possibly increased adverse CNS effects metronidazole: Risk of CNS toxicity, resulting in confusion and psychosis oral anticoagulants: Possibly increased anticoagulant effects paraldehyde: Decreased paraldehyde metabolism, increased blood paraldehyde level
phenytoin: Possibly increased blood phenytoin level and risk of phenytoin toxicity tricyclic antidepressants: Possibly temporary delirium caffeine: Possibly increased cardiovascular and CNS effects of caffeine
alcohol use: Disulfiram-alcohol reaction (if within 14 days of disulfiram therapy)

Side Efect

CNS: Drowsiness, headache, peripheral neuropathy, psychotic reaction, tiredness
EENT: Blurred vision, garlic or metallic taste, optic atrophy, optic neuritis
GU: Impotence
SKIN: Rash

Cautions

Disulfiram is given only to patients who are highly motivated to stop drinking and who are receiving psychotherapy or substance abuse counseling.

Alcohol content of patient’s other should be checked before starting therapy.
WARNING Never give drug to patient without her knowledge or who is intoxicated.

If needed, crush tablet and mix with fluids before administration.

Don’t give drug within 14 days of patient’s ingestion of alcohol-containing substance.

Expect alcohol ingestion during disulfiram therapy to produce a severe reaction that lasts from 30 minutes to several hours. Symptoms may include angina, anxiety, blurred vision, confusion, diaphoresis, dyspnea, heart failure, hypotension, nausea, palpitations, sinus tachycardia, syncope, thirst, throbbing headache, throbbing in neck, vertigo, vomiting, and weakness. A deep sleep usually follows.
WARNING Ingestion of three or more alcoholic beverages with a disulfiram dose greater than 500 mg daily may cause respiratory depression, arrhythmias, and cardiac arrest.

If patient takes phenytoin, monitor blood phenytoin level before and during disulfiram therapy, and adjust dosage of either drug as prescribed.

Interactions

may not occur if disulfiram therapy starts before phenytoin therapy. A subtherapeutic phenytoin level may result if disulfiram therapy stops.

If patient takes an oral anticoagulant, monitor PT before and during disulfiram therapy, and adjust anticoagulant dosage as prescribed. Drug interactions may not disulfiram 334 occur if disulfiram therapy starts before warfarin therapy. If disulfiram therapy stops, be prepared to adjust warfarin dosage to avoid loss of hypoprothrombinemic effects.

Expect some

Side Efect

, such as drowsiness, headache, and impotence, to subside over time or with a brief dosage reduction.

Because one-fifth of a disulfiram dose may stay in the body for 1 week or longer, alcohol ingestion may continue to produce unpleasant symptoms for up to 2 weeks after therapy stops.

Expect therapy to last months to years, depending on patient’s ability to abstain from alcohol.

PATIENT SAFTY

Teach patient’s household and family members about precautions needed and risks associated with disulfiram therapy.

Explain that drug doesn’t cure alcoholism but does help deter alcohol consumption.

If patient reports daytime drowsiness, advise her to take drug in the evening.

Warn patient to avoid alcohol-containing substances, such as vinegar, cough syrup, and sauces, during therapy because a disulfiram-alcohol reaction may occur after ingesting as little as 15 ml of 100proof alcohol. Urge her to avoid alcoholcontaining liniments and lotions as well.

Teach patient what to expect if disulfiramalcohol reaction occurs. Inform her that a deep sleep usually follows the reaction.

Advise patient that a reaction can occur up to 14 days after therapy stops and that a severe reaction may cause respiratory depression, arrhythmias, and cardiac arrest.

Instruct patient to carry medical identification that indicates drug, describes possible reactions, and lists someone to notify in case of emergency.

Category

Chemical class: Synthetic catecholamine
Therapeutic class: Cardiac stimulant

Pregnancy category: Not rated

Indications

To treat low cardiac output and heart failure
IV:
Adults. 2.5 to 10 mcg/kg/min as continuous infusion adjusted according to hemodynamic response. Children. 5 to 20 mcg/kg/min as continuous infusion adjusted according to hemodynamic response. Route Onset Peak Duration I.V. 1–2 min Unknown Under 5 min

Mechanism of Action

Mainly stimulates beta1-adrenergic receptors, and mildly stimulates beta2and alpha1-adrenergic receptors. Beta1-receptor stimulation produces a positive inotropic effect on the myocardium, increasing cardiac output by boosting myocardial contractility and stroke volume. Increased myocardial contractility raises coronary blood flow and myocardial oxygen consumption. Systolic blood pressure typically rises as a result of increased stroke volume. Other hemodynamic effects include decreased systemic vascular resistance, which reduces afterload, and decreased ventricular filling pressure, which reduces preload.

Incompatibilities

Don’t combine dobutamine with cefamandole, cefazolin, hydrocortisone sodium succinate, cephalothin, penicillin, sodium ethycrynate, and sodium heparin because of incompatibility. Don’t mix dobutamine with alkaline solutions, such as sodium bicarbonate, because of possible physical incompatibility. Don’t use diluents that contain sodium bisulfite or ethanol.

Contraindications

Hypersensitivity to dobutamine or its components, idiopathic hypertrophic subaortic stenosis

Interactions

beta blockers: Possibly increased alphaadrenergic activity and peripheral resistance bretylium: Potentiated vasopressor activity, possibly arrhythmias dobutamine hydrochloride 335 D cyclopropane, halothane: Possibly serious arrhythmias guanethidine: Decreased hypotensive effect of guanethidine, possibly resulting in severe hypertension thyroid hormones: Increased cardiovascular effects of thyroid hormones or dobutamine tricyclic antidepressants: Possibly potentiated cardiovascular and vasopressor effects of dobutamine, resulting in arrhythmias, hyperpyrexia, or severe hypertension

Side Efect

CNS: Fever, headache, nervousness, restlessness
CV: Angina, bradycardia, hypertension, hypotension, palpitations, PVCs, tachycardia
GI: Nausea, vomiting
RESP: Dyspnea
SKIN: Extravasation with tissue necrosis and sloughing, rash
Other: Hypokalemia

Cautions

Avoid giving dobutamine to patients with uncorrected hypovolemia. Expect prescriber to order whole blood or plasma volume expanders to correct hypovolemia. Also avoid giving dobutamine to patients with acute MI because it can intensify or extend myocardial ischemia.

Use drug cautiously in patients allergic to sulfites because drug may cause anaphylactic-like signs and symptoms; commercially available dobutamine injections contain sodium bisulfite. Also use drug cautiously in patients with atrial fibrillation because drug increases AV conduction. Keep in mind that patient should be adequately digitalized before administration.

Dilute concentrate with at least 50 ml compatible I.V. solution. A common dilution is 500 mg (40 ml from 250-ml bag) in 210 ml D5W or normal saline solution to yield 2,000 mcg/ml. Or dilute 1,000 mg (80 ml from 250-ml bag) in 170 ml D5W or normal saline solution to yield 4,000 mcg/ml. Adjust maximum concentration according to patient’s fluid requirements as prescribed. Don’t exceed 5,000 mcg/ml. Discard solution after 24 hours.

Inspect parenteral solution for particles and discoloration before administering it.

Give I.V. drug using an infusion pump.

Monitor blood pressure often during therapy, preferably by continuous intraarterial monitoring; systolic increase of 10 to 20 mm Hg may indicate dobutamineinduced increase in cardiac output.

If hypotension develops, expect to reduce dosage or discontinue drug.

Monitor heart rate and rhythm continuously for PVCs, which may result from drug’s stimulatory effect on heart’s conduction system, and sinus tachycardia, which results from positive chronotropic effect of beta stimulation and may increase heart rate by 5 to 15 beats/ minute.

Monitor hemodynamic parameters, such as central venous pressure, pulmonary artery wedge pressure, and cardiac output, as indicated, to assess drug’s effectiveness.
WARNING Monitor serum potassium level to check for hypokalemia, a rare result of beta2stimulation that causes electrolyte imbalance.

Monitor urine output hourly, as appropriate, to check for improved renal blood flow.

Dobutamine isn’t indicated for long-term treatment of heart failure because it may not be effective and may increase the risk of hospitalization and death.

PATIENT SAFTY

Explain the need for frequent hemodynamic monitoring.

Category

Chemical class: Anionic surfactant
Therapeutic class: Laxative, stool softener

Pregnancy category: C

Indications

To treat constipation (DOCUSATE CALCIUM) Adults and adolescents.240 mg at bedtime until bowel movements are normal. Children age 6 and over. 50 to 150 mg at bedtime. , LIQUID, SYRUP,(DOCUSATE SODIUM) Adults and adolescents.50 to 500 mg at bedtime. Children ages 6 to 12. 40 to 120 mg at bedtime. Children ages 3 to 6. 20 to 60 mg at bedtime. Children under age 3. 10 to 40 mg at bedtime. ,(DOCUSATE POTASSIUM) Adults and adolescents.100 mg t.i.d. until bowel movements are normal. Children age 6 and over.100 mg at bedtime. Route Onset Peak Duration P.O. 24–72 hr Unknown Unknown

Mechanism of Action

Acts as a surfactant that softens stool by decreasing surface tension between oil and water in feces. This action lets more fluid penetrate stool, forming a softer fecal mass.

Contraindications

Fecal impaction; hypersensitivity to docusate salts or their components; intestinal obstruction; nausea, vomiting, or other symptoms of appendicitis; undiagnosed abdominal pain

Interactions

mineral oil: Increased mineral oil absorption, increased risk of toxicity tetracycline: Decreased tetracycline absorption

Side Efect

CNS: Dizziness, syncope
CV: Palpitations
GI: Abdominal cramps and distention, diarrhea, nausea, perianal irritation, vomiting
MS: Muscle weakness

Cautions

WARNING Expect long-term or excessive use of docusate to cause dependence on laxatives for bowel movements, electrolyte imbalances, osteomalacia, steatorrhea, and vitamin and mineral deficiencies.

Assess for laxative abuse syndrome, especially in women with depression, personality disorders, or anorexia nervosa.

PATIENT SAFTY

Tell patient not to use docusate when she has abdominal pain, nausea, or vomiting.

Advise patient to take docusate with a full glass of water or milk.

To help prevent constipation, encourage patient to increase fiber intake, exercise regularly, and drink 6 to 8 glasses (240 ml/ glass) of water daily.

Instruct patient to notify prescriber about rectal bleeding; symptoms of electrolyte imbalances, such as dizziness, light-headedness, muscle cramping, and weakness; and unrelieved constipation.

Category

Chemical class: Methanesulfonanilide derivative
Therapeutic class: Class III antiarrhythmic

Pregnancy category: C

Indications

To convert symptomatic atrial fibrillation or flutter to normal sinus rhythm or to maintain normal sinus rhythm in patients converted from symptomatic atrial fibrillation or flutter
Adults. Initial: 500 mcg b.i.d. for patients with creatinine clearance above 60 ml/min/ 1.73 m2. Maintenance: Dosage based on QTc interval. If, 2 to 3 hr after initial dose, QTc interval increase is 15% of baseline or less, initial dose given b.i.d. Maximum: 500 mcg b.i.d. dofetilide 337 D
DOSAGE ADJUSTMENT Initial dose reduced to 250 mcg b.i.d. if creatinine clearance is 40 to 60 ml/min/1.73 m2and to 125 mcg b.i.d. if clearance is 20 to 39 ml/min/ 1.73 m2, as prescribed. If, 2 to 3 hr after initial dose, QTc interval has increased by at least 15% or is more than 500 milliseconds (msec) (550 msec in patients with ventricular conduction abnormalities), dosage decreased by 50%, as prescribed. However, for patients receiving lowest initial dose of 125 mcg b.i.d., dosage reduced to 125 mcg daily, as prescribed. During next four doses (given every 2 to 3 hr, as prescribed), if QTc interval increases to more than 500 msec (550 msec in patients with ventricular conduction abnormalities), expect to discontinue drug, as prescribed. Route Onset Peak Duration P.O. Unknown 2 hr 4 hr

Mechanism of Action

Selectively blocks potassium channels in myocardial cell membranes involved in cardiac repolarization. By blocking potassium channels, dofetilide prolongs ventricular refractoriness (widens QT interval), effective refractory period, and action potential duration. These actions terminate or prevent reentrant tachyarrhythmias, such as atrial fibrillation, atrial flutter, and ventricular tachycardia.

Contraindications

Cardiac conduction disturbances without an artificial pacemaker; congenital or acquired QT prolongation syndrome; concurrent therapy with cimetidine, hydrochlorothiazide, ketoconazole, trimethoprim, or verapamil; hypersensitivity to dofetilide or its components; severe renal impairment (creatinine clearance less than 20 ml/min/ 1.73 m2)

Interactions

amiloride, cimetidine, co-trimoxazole, ketoconazole, megestrol, metformin, triam-terene, trimethoprim: Possibly increased blood dofetilide level azole antifungals, diltiazem, nefazodone, norfloxacin, protease inhibitors, quinine, selective serotonin reuptake inhibitors, zafirlukast: Possibly increased blood dofetilide level and risk of dofetilide toxicity bepridil, cisapride, macrolide antibiotics, phenothiazines, tricyclic antidepressants: Possibly prolonged QT interval class I and III antiarrhythmics, especially amiodarone: Possibly prolonged QT interval and increased risk of dofetilide-induced proarrhythmias diuretics (potassium-depleting): Increased risk of torsades de pointes in patients with hypokalemia or hypomagnesemia hydrochlorothiazide, verapamil: Possibly increased blood dofetilide level and increased risk of torsades de pointes grapefruit juice: Increased dofetilide level marijuana use: Increased dofetilide level

Side Efect

CNS: Cerebral ischemia, dizziness, facial or flaccid paralysis, headache, insomnia, paresthesia, slurred speech, stroke, syncope
CV: AV block, bradycardia, cardiac arrest, chest pain, edema, MI, tachycardia, ventricular arrhythmias (including torsades de pointes and ventricular tachycardia)
GI: Abdominal pain, diarrhea, hepatic dysfunction, nausea
MS: Back pain, muscle weakness
RESP: Cough, dyspnea, respiratory tract infection
SKIN: Jaundice, rash
Other: Angioedema, flulike symptoms, weight gain

Cautions

WARNING If patient has previously received amiodarone, be aware that dofetilide shouldn’t be started until blood amiodarone level is less than 0.3 mcg/ml or until amiodarone has been withdrawn for at least 3 months.

Evaluate and document QTc interval before and during dofetilide therapy.

Place patient on continuous ECG monitoring for at least 3 days, as ordered, during dofetilide therapy.
WARNING If patient does not convert to normal sinus rhythm within 24 hours of starting dofetilide, expect possible synchronized electrical cardioversion.

Be prepared to reevaluate renal function and QTc interval every 3 months, as ordered, during dofetilide therapy.

When switching to dofetilide from class I or class III antiarrhythmics, or after withdrawing antiarrhythmic treatment, monitor continuous ECG for at least 30 hours, as ordered.

If patient requires a drug that may interact with dofetilide, expect to discontinue dofetilide, as prescribed, for 2 or more days before starting the other drug.
WARNING Monitor laboratory test results for hypokalemia or hypomagnesemia, especially in patients taking diuretics, because of the increased risk of dofetilideinduced torsades de pointes.

Monitor women often for adverse reactions, including prolonged QTc interval and torsades de pointes; they have 12% to 18% lower renal clearance of drug than men and therefore a greater risk of adverse reactions.

PATIENT SAFTY

Advise patient to swallow dofetilide capsules with water.

Instruct patient to avoid drinking grapefruit juice while taking this drug.

Inform patient that she may be hospitalized for at least 3 days if dofetilide dosage is increased.

Teach patient to measure pulse rate and blood pressure during dofetilide therapy.

Urge patient to report chest discomfort, fluttering, or palpitations immediately.

Advise patient to consult prescriber before using any OTC , nutritional supplements, or herbal products.

Instruct patient to keep follow-up appointments to monitor heart rhythm.

Category

Chemical class: Carboxylate monomethanesulfonate
Therapeutic class: Antiemetic

Pregnancy category: B

Indications

To prevent nausea and vomiting due to chemotherapy

ORALL

, Adults and children over age 16. 100 mg within 1 hr before chemotherapy. Children ages 2 to 16. 1.8 mg/kg within 1 hr before chemotherapy. Maximum: 100 mg.
I.V.INJECTION Adults and children over age 16. 1.8 mg/kg or 100 mg as a single dose within 30 min before chemotherapy. Children ages 2 to 16. 1.8 mg/kg as a single dose within 30 min before chemotherapy. Maximum: 100 mg. To prevent postoperative nausea and vomiting

ORALL

, Adults and children over age 16. 100 mg within 2 hr before surgery. Children ages 2 to 16. 1.2 mg/kg within 2 hr before surgery. Maximum: 100 mg.
I.V.INJECTION Adults and children over age 16. 12.5 mg 15 min before end of anesthesia. Children ages 2 to 16. 0.35 mg/kg 15 min before end of anesthesia. Maximum: 12.5 mg/dose. To treat postoperative nausea and vomiting
I.V.INJECTION Adults and children over age 16. 12.5 mg as single dose as soon as symptoms develop. Children ages 2 to 16. 0.35 mg/kg as single dose as soon as symptoms develop. Maximum: 12.5 mg/dose.

Mechanism of Action

With its active metabolite hydrodolasetron, prevents activation of serotonin 5-HT3 receptors located peripherally on vagal nerve terminals and centrally in chemoreceptor trigger zone, thereby decreasing the vomiting reflex.

Contraindications

Hypersensitivity to dolasetron or components

Interactions

atenolol: Possibly decreased dolasetron clearance
cimetidine: Possibly increased blood dolasetron level
rifampin: Possibly decreased blood dolasetron level

Side Efect

CNS: Headache
CV: Cardiac arrest, hypertension, hypotension, MI, ventricular fibrillation and tachydolasetron mesylate 339 D cardia, wide-complex tachycardia
GI: Diarrhea
SKIN: Rash
Other: Injection site pain

Cautions

Expect to give up to 100 mg of dolasetron I.V. in 30 seconds or to dilute it in normal saline solution, D5W, dextrose 5% in halfnormal (0.45) saline solution, or lactated Ringer’s solution and infuse for up to 15 minutes, as prescribed.

Flush I.V. line with compatible solution before and after drug administration.

Expect to prepare an oral solution of dolasetron for patients unable to swallow tablets by diluting injection solution with apple or apple-grape juice.
WARNING Assess patient for ECG changes, including prolonged PR, QTc, and QT intervals and widened QRS complex.

PATIENT SAFTY

For children or patients who have trouble swallowing, explain that oral solution can be prepared by diluting injection form of drug with apple or apple-grape juice.

Inform patient that oral solution may be refrigerated for up to 48 hours but should be discarded after 2 hours at room temperature.

Category

Chemical class: Piperidine derivative
Therapeutic class: Antidementia

Pregnancy category: C

Indications

To treat dementia of Alzheimer’s type

ORALL

,
Adults. Initial: 5 mg at bedtime. After 4 to 6 wk, dosage increased to 10 mg at bedtime, as indicated. Maximum: 10 mg daily.

Mechanism of Action

Reversibly inhibits acetylcholinesterase and improves acetylcholine’s concentration at cholinergic synapses. Raising acetylcholine level in the cerebral cortex may improve cognition. Donepezil becomes less effective as Alzheimer’s disease progresses and number of intact cholinergic neurons declines.

Contraindications

Hypersensitivity to donepezil, piperidine derivatives, or their components

Interactions

anticholinergics: Possibly interference with activity of these carbamazepine, dexamethasone, phenobarbital, phenytoin,
rifampin: Increased donepezil elimination rate cholinergic agonists, neuromuscular blockers: Possibly synergistic effects of these ketoconazole,
quinidine: Inhibited donepezil metabolism
NSAIDs: Possibly increased gastric acid secretion and increased risk of GI bleeding

Side Efect

CNS: Abnormal gait, agitation, anxiey, asthenia, depression, dizziness, dream disturbances, fatigue, fever, headache, hostility, insomnia, nervousness, seizures, somnolence, syncope, tremor
CV: Abnormal ECG, bradycardia, chest pain, edema, heart failure, hypertension, hypotension
EENT: Pharyngitis
ENDO: Hyperglycemia
GI: Abdominal pain, anorexia, constipation, diarrhea, dyspepsia, gastroenteritis, fecal incontinence, nausea, vomiting
GU: Cystitis, glycosuria, hematuria, urinary frequency or incontinence, UTI
HEME: Anemia, hemorrhage
MS: Arthralgia, back pain, elevated creatine kinase level, muscle spasms
RESP: Bronchitis, increased cough, pneumonia
SKIN: Ecchymosis, eczema, pruritus, rash, ulceration
Other: Angioedema, dehydration, elevated alkaline phosphatase or lactate dehydrogenase level, flu syndrome, weight loss

Cautions

Use donepezil cautiously in patients with bladder obstruction because drug’s weak peripheral cholinergic effect could obstruct outflow.

Use drug cautiously in patients with asthma, COPD, or other pulmonary disorders because it has weak affinity for peripheral donepezil hydrochloride 340 cholinesterase, which may increase bronchoconstriction and bronchial secretions.

If patient has cardiac disease, monitor heart rate and rhythm for bradycardia, which may result from increased vagal tone caused by drug’s inhibition of peripheral cholinesterase. Reduced heart rate may be especially significant if patient has sick sinus syndrome, bradycardia, or other supraventricular arrhythmia.

Take safety precautions if patient is dizzy or has other adverse CNS reactions.

PATIENT SAFTY

Advise patient to take donepezil just before going to bed.

Inform her that drug may be taken with or without food.

Instruct patient to avoid hazardous activities, such as driving, until drug’s CNS effects are known. Urge her to take safety precautions to prevent falling if she has

Side Efect

, such as dizziness.

If patient has a history of peptic ulcer disease or gastric irritation, explain that drug may aggravate these conditions by increasing gastric acid secretion.

Caution patient to avoid NSAIDs during therapy because of risk of GI bleeding. Urge her to notify prescriber immediately if she notices black, tarry stools.

Category

Chemical class: Catecholamine
Therapeutic class: Cardiac stimulant, vasopressor

Pregnancy category: C

Indications

To correct hypotension that’s unresponsive to adequate fluid volume replacement or occurs as part of shock syndrome caused by bacteremia, chronic cardiac decompensation, drug overdose, MI, open-heart surgery, renal failure, trauma, or other major systemic illnesses; to improve low cardiac output
IV:
Adults.0.5 to 3 mcg/kg/min for vasodilation of renal arteries; 2 to 10 mcg/kg/min for positive inotropic effects and increased cardiac output; 10 mcg/kg/min, increased gradually according to patient’s response, for increased systolic and diastolic blood pressures.
DOSAGE ADJUSTMENT Initial dosage reduced to 10% of usual amount if patient has taken MAO inhibitor in previous 2 to 3 wk. Children.1 to 5 mcg/kg/min increased gradually in increments of 2.5 to 5 mcg/kg/min to achieve desired results. Maximum: 20 mcg/kg/min. Route Onset Peak Duration I.V. In 5 min Unknown Up to 10 min

Mechanism of Action

Stimulates dopamine1(D1) and dopamine2 (D2) postsynaptic receptors. D1receptors mediate vasodilation in renal, mesenteric, coronary, and cerebral blood vessels. D2 receptors inhibit norepinephrine release. In higher doses, dopamine also stimulates alpha1and alpha2receptors, causing vascular smooth-muscle contraction. At doses of 0.5 to 3 mcg/kg/min, this naturally occurring catecholamine mainly affects dopaminergic receptors in renal, mesenteric, coronary, and cerebral vessels, resulting in vasodilation, increased renal blood flow, improved GFR, and increased urine output. At doses of 2 to 10 mcg/kg/ min, dopamine stimulates beta1-adrenergic receptors, increasing cardiac output while maintaining dopaminergic-induced vasodilation. At doses of 10 mcg/kg/min or more, alpha-adrenergic agonism takes over, causing increased peripheral vascular resistance and renal vasoconstriction.

Incompatibilities

Don’t add dopamine to 5% sodium bicarbonate, alkaline I.V. solutions, oxidizing agents, or iron salts.

Contraindications

Pheochromocytoma, uncorrected ventricular fibrillation, ventricular tachycardia, and other tachyarrhythmias

Interactions

alpha blockers, haloperidol, loxapine, phenothiazines,
thioxanthenes: Antagonized dopamine hydrochloride 341 D peripheral vasoconstriction with high doses of dopamine anesthetics, such as chloroform, enflurane, halothane, isoflurane, and
methoxyflurane: Increased risk of severe atrial and ventricular arrhythmias antihypertensives, diuretics used as antihypertensives: Possibly decreased antihypertensive effects of these
beta blockers: Antagonized beta receptor– mediated inotropic effects of dopamine digitalis glycosides: Possibly increased risk of arrhythmias and additive inotropic effects diuretics: Possibly increased diuretic effects of dopamine or diuretic doxapram: Possibly increased vasopressor effects of dopamine or doxapram ergot alkaloids: Enhanced peripheral vasoconstriction guanadrel, guanethidine: Possibly decreased hypotensive effects of these and potentiated vasopressor response to dopamine, resulting in hypertension and arrhythmias levodopa: Increased risk of arrhythmias
MAO inhibitors: Prolonged and intensified cardiac stimulation and vasopressor effect maprotiline, tricyclic antidepressants: Possibly potentiated cardiovascular and vasopressor effects of dopamine, resulting in arrhythmias, hyperpyrexia, or severe hypertension mecamylamine, methyldopa: Possibly decreased hypotensive effects of these and enhanced vasopressor effect of dopamine
methylphenidate: Possibly potentiated vasopressor effect of dopamine nitrates: Possibly decreased antianginal effects of nitrates; possibly decreased vasopressor effect of dopamine, resulting in hypotension oxytocic : Possibly severe hypertension phenoxybenzamine: Possibly antagonized peripheral vasoconstriction of dopamine, causing hypotension and tachycardia
phenytoin: Possibly sudden bradycardia and hypotension rauwolfia alkaloids: Possibly decreased hypotensive effects of these sympathomimetics: Possibly increased adverse cardiovascular and other effects thyroid hormones: Increased risk of coronary insufficiency

Side Efect

CNS: Headache
CV: Angina, bradycardia, hypertension, hypotension, palpitations, peripheral vasoconstriction, sinus tachycardia, ventricular arrhythmias
GI: Nausea, vomiting
RESP: Dyspnea
SKIN: Extravasation with tissue necrosis

Cautions

If possible, avoid giving dopamine to patients with occlusive vascular disease, such as atherosclerosis, Buerger’s disease, diabetic endarteritis, or Raynaud’s disease, because of risk of decreased peripheral circulation.

Use drug cautiously in patients with cardiac disease, particularly coronary artery disease, because dopamine increases myocardial oxygen demand. Also use drug cautiously in patients allergic to sulfites, which are contained in some forms of dopamine.

Inspect parenteral solution for particles and discoloration before administration.

Dilute dopamine concentrate with a compatible I.V. solution before administering. Typical dilution is 400 mg in 250 ml to yield 1.6 mg/ml. Don’t exceed 3.2 mg/ml.

If patient has hypovolemia, ensure adequate fluid resuscitation before giving drug.

Give drug by I.V. infusion using an infusion pump.
WARNING When infusion rate exceeds 20 mcg/kg/min, monitor patient for excessive vasoconstriction and loss of renal vasodilating effects. Avoid using an infusion rate above 50 mcg/kg/min.

If you must infuse more than 20 mcg/kg/ min of dopamine to maintain blood pressure, expect to infuse norepinephrine as prescribed.

To avoid extravasation and tissue necrosis, administer infusion through a central catheter. If you must give drug via peripheral line, inspect site often for signs of extravasation and necrosis. If you detect such signs, start a new I.V. line for dopamine infusion, discontinue previous I.V. line, and notify prescriber immediately.

If drug extravasates, expect to give 5 to 10 mg phentolamine diluted in 10 to 15 ml dopamine hydrochloride 342 normal saline solution, as prescribed. Phentolamine infiltrates directly into area to antagonize vasoconstriction and minimize sloughing and tissue necrosis.

Titrate dopamine gradually to minimize hypotension, especially after a high infusion rate.

Monitor blood pressure continuously with an intra-arterial line, as indicated.

Place patient on continuous ECG monitoring, and assess heart rate and rhythm for arrhythmias.

Monitor patient’s hemodynamic parameters, such as central venous pressure, pulmonary artery wedge pressure, and cardiac output, as indicated, to assess effectiveness of dopamine therapy.

Monitor urine output hourly as appropriate to assess patient for improved renal blood flow.

PATIENT SAFTY

Explain the need for frequent hemodynamic monitoring.

Category

Chemical class: Carbapenem
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat complicated intra-abdominal infections caused by Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Bacteroides caccae, B. fragilis, B. thetaiotaomicron, B. uniformis, B. vulgatus, Streptococcus intermedius, S. constellatus, and Peptostreptococcus micros and complicated UTIs, including pyelonephritis caused by E. coli, K. pneumoniae, Proteus mirabilis, P. aeruginosa, and Acinetobacter baumannii
IV:
Adults.500 mg infused over 1 hr every 8 hr for 5 to 14 days. May switch to oral therapy if improvement after 3 days.
DOSAGE ADJUSTMENT For patients with impaired renal function or creatinine clearance of 30 to 50 ml/min/1.73 m2, dosage reduced to 250 mg infused over 1 hr every 8 hr. For creatinine clearance of 10 to 30 ml/min/1.73 m2, dosage reduced to 250 mg infused over 1 hr every 12 hr. Route Onset Peak Duration I.V. Unknown 1 hr 8 hr

Mechanism of Action

Inhibits cell wall synthesis in susceptible bacteria. Doripenem inactivates multiple penicillin-binding proteins essential in cell wall synthesis to cause cell death.

Incompatibilities

Don’t mix doripenem with other or add to solutions containing other because of potential for incompatibility.

Contraindications

History of anaphylactic reactions to betalactams; hypersensitivity to doripenem, its components or other carbapenems

Interactions

divalproex sodium,
valproic acid: Decreased effectiveness of valproic acid with possible loss of seizure control probenecid: Increased plasma concentrations of doripenem

Side Efect

CNS: Headache, seizure
CV: Phlebitis
EENT: Oral candidiasis
GI: Diarrhea, liver enzyme elevation, nausea
GU: Vaginitis
HEME: Leukopenia, neutropenia
SKIN: Dermatitis, erythema, erythema multiforme, macular or papular eruptions, pruritus, rash, Stevens Johnson Syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis

Cautions

Use cautiously in patients with a history of hypersensitivity to cephaloporins or penicillins because cross sensitivity may occur.

Constitute vial with 10 ml sterile water for injection or normal saline solution, and gently shake to form a suspension. Withdraw suspension using a syringe with a 21G needle and add it to an infusion bag containing 100 ml normal saline solution or 5% dextrose. Gently shake until clear. If administering reduced dosage of 250 mg, doripenem 343 D remove 55 ml of prepared solution from infusion bag and discard before infusion.

Be aware that upon constitution, suspension in the vial must be diluted within 1 hour. Once drug is diluted in infusion solution, drug stored at room temperature must be used within 8 hours if mixed in normal saline solution and within 4 hours if mixed in 5% dextrose. If infusion solution is refrigerated, it must be used within 24 hours or discarded.

Monitor patient closely for evidence of hypersensitivity, especially if patient has multiple allergies, because serious and occasionally fatal hypersensitivity reactions have occurred in patients receiving beta-lactam antibiotics. If an allergic reaction occurs, discontinue drug immediately, notify prescriber, and expect to administer emergency treatment such as epinephrine, oxygen, I.V. fluids, I.V. antihistamines, corticosteroids, and pressor amines, as ordered, and provide airway management.

Assess patient’s bowel pattern daily; severe diarrhea may be caused by Clostridium difficile. If suspected, expect to stop drug and provide treatment as prescribed.

PATIENT SAFTY

Instruct patient to report any evidence of allergic reaction, such as rash, hives, itching or trouble breathing.

Advise patient to report diarrhea if severe or persistent.

Category

Chemical class: Pyrrolidinone derivative
Therapeutic class: Respiratory stimulant

Pregnancy category: B

Indications

To stimulate respiration in COPDrelated acute respiratory insufficiency
IV: Adults and adolescents. 1 to 2 mg/min titrated according to respiratory response. Maximum: 3 mg/min for up to 2 hr. To treat respiratory depression after anesthesia
IV: Adults and adolescents.5 mg/min until desired response occurs and then reduced to 1 to 3 mg/min. Maximum: Cumulative dose of 4 mg/kg or 300 mg.
I.V.INJECTION Adults and adolescents.0.5 to 1 mg/kg, repeated every 5 min, if needed. Maximum: 1.5 mg/kg as a single dose or 2 mg/kg every 5 min. Route Onset Peak Duration I.V. 20–40 sec 1–2 min 5–12 min

Mechanism of Action

Activates peripheral carotid, aortic, and other chemoreceptors to stimulate respiration, resulting in increased tidal volume and respiratory rate. Doxapram also may increase respiratory rate and tidal volume by directly stimulating the respiratory center in the medulla oblongata.

Incompatibilities

To avoid precipitation and gas formation, don’t mix doxapram with alkaline solutions, such as aminophylline, sodium bicarbonate, or 2.5% thiopental.

Contraindications

Age less than 1 month; cerebral edema; head injury; hypersensitivity to doxapram or its components; mechanical disorders of ventilation, including acute bronchial asthma, flail chest, muscle paresis, obstruction, pneumothorax, and pulmonary fibrosis; pulmonary embolism; seizure disorder; severe cardiovascular disorder; severe hypertension; stroke; uncompensated heart failure

Interactions

chloroform, cyclopropane, enflurane, halothane, isoflurane, methoxyflurane, trichloroethylene: Possibly adverse myocardial effects if doxapram given within 10 minutes of these CNS stimulants: Possibly excessive CNS stimulation, with arrhythmias, insomnia, irritability, nervousness, or seizures MAO inhibitors, sympathomimetics: Additive vasopressor effects skeletal muscle relaxants: Masked residual effects of muscle relaxants doxapram hydrochloride 344

Side Efect

CNS: Disorientation, dizziness, headache
CV: Arrhythmias, including sinus tachycardia; hypertension
GI: Diarrhea, hiccups, nausea, vomiting
GU: Urine retention
RESP: Bronchospasm, cough, dyspnea
SKIN: Diaphoresis
Other: Injection site pain, redness, swelling, and thrombophlebitis

Cautions

Avoid giving doxapram to patients receiving mechanical ventilation.

Maintain a patent airway, and assess for optimal oxygenation before giving drug.

Monitor I.V. insertion site for extravasation and signs of thrombophlebitis or local skin irritation.

If hypertension or dyspnea develops suddenly, stop infusion as directed.

Assess patient for early signs and symptoms of overdose, including enhanced deep tendon reflexes, skeletal muscle hyperactivity, and tachycardia.

PATIENT SAFTY

Explain the need for frequent pulse and blood pressure monitoring.

Category

Chemical class: Quinazoline derivative
Therapeutic class: Antihypertensive, benign prostatic hyperplasia therapeutic agent

Pregnancy category: C

Indications

To manage hypertension
Adults.Initial: 1 mg daily. Doubled every 1 to 2 wk, if needed to achieve desired blood pressure. Maximum: 16 mg daily. To treat benign prostatic hyperplasia (BPH)
Adults. Initial: 1 mg daily. Doubled every 1 to 2 wk, if needed, based on signs and symptoms. Maximum: 8 mg daily.

Mechanism of Action

Competitively inhibits alpha1-adrenergic receptors in the sympathetic nervous system, causing peripheral vasodilation and reduced peripheral vascular resistance. This action increases heart rate and decreases blood pressure, especially when the patient stands. Doxazosin also relaxes smooth muscle of the bladder neck, prostate, and prostate capsule, which reduces urethral resistance and pressure and urinary outflow resistance. Route Onset Peak Duration P.O. 1–2 hr* 2–6 hr 24 hr

Contraindications

Hypersensitivity to doxazosin, prazosin, terazosin, or their components

Interactions

antihypertensives, diuretics, phosphodiesterase-5 inhibitors: Enhanced hypotensive effects
cimetidine: Possibly increased blood doxazosin level dopamine: Antagonized vasopressor effect of high-dose dopamine ephedrine, metaraminol, methoxamine, phenylephrine: Possibly decreased vasopressor effects of these epinephrine: Possibly severe hypotension and tachycardia
NSAIDs: Possibly loss of hypotensive activity from sodium or fluid accumulation

Side Efect

CNS: Dizziness, drowsiness, headache, nervousness, restlessness, vertigo
CV: Arrhythmias, including sinus tachycardia; first-dose orthostatic hypotension; palpitations; peripheral edema
EENT: Intraoperative floppy iris syndrome, rhinitis
GI: Nausea
RESP: Dyspnea

Cautions

Don’t give drug to hypotensive patients.

Use doxazosin cautiously in patients with hepatic disease (because normal dosage may cause exaggerated effects) and in elderly patients (because hypotensive response may be more pronounced). doxazosin mesylate 345 D * For hypertension; in 2 wk for BPH. For hypertension; unknown for BPH.
WARNING Monitor patient for orthostatic hypotension (which may cause syncope) early in therapy, especially after exercise and in patients with hypovolemia.

Monitor blood pressure for 2 to 6 hours after first dose and with each increase because orthostatic hypotension commonly occurs at this time. Adjust dose as prescribed, based on standing blood pressure.

Carefully monitor patients with renal disease for exaggerated effects, such as firstdose orthostatic hypotension.

Monitor urination, checking for difficulty urinating and urine retention, to assess drug’s effects on BPH.

PATIENT SAFTY

Inform patient that she may take doxazosin in the morning or evening and with food, if desired.

Instruct patient to change position slowly to minimize orthostatic hypotension.

Advise patient to avoid standing for long periods, exercising, using alcohol, and going outside in hot weather; these activities may worsen orthostatic hypotension.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Category

Chemical class: Dibenzoxepin derivative
Therapeutic class: Antidepressant

Pregnancy category: Not rated

Indications

To treat mild to moderate depression or anxiety , Adults and adolescents. 75 to 150 mg daily at bedtime. Maximum: 150 mg daily. To treat mild to moderate depression or anxiety with organic disease , Adults and adolescents. 25 to 50 mg daily. To treat severe depression or anxiety , Adults and adolescents. 50 mg t.i.d., gradually increased to 300 mg daily, as indicated.

Mechanism of Action

May block serotonin and norepinephrine reuptake by adrenergic nerves. In this way, the tricyclic antidepressant raises serotonin and norepinephrine levels at nerve synapses, which may elevate mood and reduce depression. Route Onset Peak Duration P.O. 2–3 wk Unknown Unknown

Incompatibilities

Don’t mix doxepin solution with carbonated beverages or grape juice.

Contraindications

Acute recovery phase of MI; concurrent use of MAO inhibitor; glaucoma; hypersensitivity to doxepin, other tricyclic antidepressants, or their components; urine retention

Interactions

amantadine, anticholinergics, antidyskinetics, antihistamines: Possibly intensified anticholinergic effects, causing confusion, hallucinations, and nightmares anticonvulsants: Possibly lowered seizure threshold and decreased effects of these antithyroid : Possibly increased risk of agranulocytosis barbiturates, carbamazepine: Increased doxepin metabolism, decreased blood doxepin level, possibly lowered seizure threshold bupropion, clozapine, cyclobenzaprine, haloperidol, loxapine, maprotiline, molindone, phenothiazines,
thioxanthenes: Possibly prolonged and intensified sedative and anticholinergic effects of either drug, possibly increased risk of seizures cimetidine, flecainide, phenothiazines, propafenone, quinidine, selective serotonin reuptake inhibitors, tricyclic antidepressants: Increased blood doxepin level from inhibited systemic clearance, resulting in increased risk of toxicity clonidine, guanadrel, guanethidine: Increased risk of hypertension, especially during second week of doxepin therapy
CNS depressants: Possibly potentiated CNS depression, hypotension, and respiratory depression corticosteroids: Possibly worsened depression doxepin hydrochloride 346 direct-acting sympathomimetics, such as epinephrine and norepinephrine: Potentiated effects of these disulfiram: Possibly transient delirium fluoxetine: Possibly increased blood doxepin level
MAO inhibitors: Possibly hyperpyrexia, hypertension, seizures, and death oral anticoagulants: Possibly increased anticoagulant effects of these pimozide: Increased risk of arrhythmias probucol: Possibly prolonged QT interval, increased risk of ventricular tachycardia thyroid hormones: Possibly increased therapeutic and toxic effects of both tolazamide: Possibly severe hypoglycemia
alcohol use: Possibly enhanced CNS depression, hypotension, and respiratory depression

Side Efect

CNS: Confusion, delirium, dream disturbances, drowsiness, fatigue, hallucinations, headache, nervousness, parkinsonism, restlessness, sedation, seizures, suicidal ideation (children and teens), tremor
CV: ECG changes, orthostatic hypotension, palpitations
EENT: Blurred vision, dry mouth, taste perversion
GI: Constipation, diarrhea, heartburn, ileus, increased appetite, nausea, vomiting,
GU: Decreased libido, ejaculation disorders
SKIN: Diaphoresis, jaundice
Other: Weight gain

Cautions

If desired, mix oral solution in 120 ml of water; milk; or orange, grapefruit, tomato, or pineapple juice.

Expect to observe

Side Efect

within a few hours after giving drug.

Evaluate patient for therapeutic response, such as decreased anxiety, apprehension, depression, fear, guilt, somatic symptoms, and worry; increased energy; and more restful sleep.
WARNING Monitor children and teens closely for evidence of suicidal thinking and behavior because doxepin increases the risk in these groups.

Keep in mind that abrupt withdrawal of doxepin after prolonged therapy can cause cholinergic rebound effects, including diarrhea, nausea, and vomiting.

Plan to discontinue drug, as prescribed, several days before elective surgery to avoid hypertension.

Monitor elderly patients for parkinsonism, especially with high-dose therapy.

Be alert for seizures. Patients with seizure disorder may need increased anticonvulsant dosage to maintain seizure control.

For patients with asthma or sulfite sensitivity, doxepin tablets may aggravate asthma or cause allergic reactions because they contain sulfites.

Follow diabetic patient’s serum glucose level closely; drug may alter glucose metabolism.

If patient takes a thyroid hormone, be alert for increased responses to both and, possibly, exaggerated drug-induced effects, such as arrhythmias and CNS stimulation. Untreated hypothyroidism prevents adequate response to therapy.

PATIENT SAFTY

WARNING Alert parents to watch their child or teen closely for abnormal thinking or behavior and increased aggression or hostility. Stress importance of notifying prescriber about unusual changes.

Instruct patient to avoid alcohol during doxepin therapy because mental alertness may decrease.

Advise diabetic patient to measure serum glucose level more often than usual.

Category

Chemical class: Fat-soluble vitamin D analogue
Therapeutic class: Antihyperparathyroid drug

Pregnancy category: B

Indications

To reduce elevated intact parathyroid hormone (iPTH) serum level when managing secondary hyperparathyroidism in patients undergoing chronic hemodialysis
Adults. Initial: 10 mcg 3 times/wk (about doxercalciferol 347 D every other day) before, during, or after dialysis. Maintenance: If iPTH level is decreased by 50% and above 300 picograms (pg)/ml, dosage increased by 2.5 mcg at 8wk intervals, as needed. If iPTH level is 150 to 300 pg/ml, initial dosage maintained. If iPTH level is less than 100 pg/ml, drug stopped for 1 wk and then restarted at a dose at least 2.5 mcg less than previous dose. Maximum: 20 mcg 3 times/wk for a total of 60 mcg/wk. To reduce elevated iPTH blood level when managing secondary hyperparathyroidism in patients with stage 3 or 4 chronic renal disease
Adults.1 mcg daily. Maintenance: If iPTH level exceeds 70 pg/ml for stage 3 or 110 pg/ ml for stage 4, dosage increased by 0.5 mcg at 2-wk intervals, as needed. If iPTH level is 35 to 70 pg/ml for stage 3 or 70 to 110 pg/ ml for stage 4, dosage is maintained. If iPTH level is less than 35 pg/ml for stage 3 or less than 70 pg/ml for stage 4, drug is stopped for 1 wk and then restarted at a dose at least 0.5 mcg lower than previous dose. Maximum: 3.5 mcg daily.

Mechanism of Action

Undergoes hepatic conversion to an active metabolite (1,25-dihydroxyvitamin D2 [1,25-dihydroxyergocalciferol]), which increases intestinal absorption of dietary calcium and renal tubular reabsorption of urinary calcium. Together with parathyroid hormone, doxercalciferol also mobilizes calcium from bone. These effects serve to maintain blood calcium levels in patients with chronic renal failure, which in turn prevents hyperparathyroidism. In patients with renal failure, decreased metabolic activation of vitamin D in the kidneys leads to chronic hypocalcemia. The parathyroid gland compensates by increasing PTH secretion, but renal failure prevents it from achieving a normal serum calcium level. Thus, secondary hyperparathyroidism develops. Because doxercalciferol doesn’t require renal conversion to form its active metabolite, it can regulate the serum calcium level and thus suppress PTH secretion and reduce its serum level in patients with chronic renal failure. An elevated PTH level in these patients leads to metabolic bone disease, such as renal osteodystrophy.

Contraindications

Evidence of vitamin D toxicity, hypersensitivity to doxercalciferol or its components, risk or history of hypercalcemia or hyperphosphatemia

Interactions

antacids that contain magnesium: Possibly additive drug effects and increased risk of hypermagnesemia cholestyramine, mineral oil, orlistat, other that affect lipid absorption: Possibly decreased doxercalciferol absorption glutethimide, phenobarbital: Possibly increased doxercalciferol metabolism and risk of

Side Efect

erythromycin,
ketoconazole: Possibly inhibited doxercalciferol metabolism and decreased effectiveness vitamin D and its analogues: Possibly additive effects, resulting in increased adverse effects, such as hypercalcemia

Side Efect

CNS: Depression, dizziness, headache, insomnia, malaise, paresthesia
CV: Bradycardia, chest pain, peripheral edema
EENT: Rhinitis
ENDO: Oversuppression of iPTH
GI: Anorexia, constipation, indigestion, nausea, vomiting
HEME: Anemia
MS: Hypertonia
RESP: Cough, dyspnea
SKIN: Pruritus
Other: Dehydration, hypercalcemia, hypercalciuria, hyperphosphatemia, weight gain

Cautions

WARNING Be aware that patients who take vitamin D should not also take doxercalciferol because they may develop severe vitamin D toxicity and hypercalcemia.

Be alert for signs and symptoms of vitamin D toxicity and hypercalcemia in patients receiving high-dose or long-term doxercalciferol therapy. Early signs and symptoms include bone pain, constipation, dry mouth, headache, metallic taste, myalgia, nausea, somnolence, vomiting, and weakness. Late signs and symptoms include albuminuria, anorexia, arrhythmias, azotemia, conjunctivitis (calcific), decreased libido, elevated AST and ALT doxercalciferol 348 levels, elevated BUN level, generalized vascular calcification, hypercholesterolemia, hypertension, hyperthermia, irritability, mild metabolic acidosis, nephrocalcinosis, nocturia, pancreatitis, photophobia, polydipsia, polyuria, pruritus, rhinorrhea, and weight loss.

Keep emergency equipment readily available in case patient develops toxicity.

Expect to monitor patient’s blood iPTH, calcium, and phosphorus levels before starting drug and weekly early in therapy.

For patients with renal failure who are having hemodialysis, oral calcium-based or other non–aluminum-containing phosphate binders and a low-phosphate diet typically are used to control serum phosphorus level. An elevated serum phosphorus level worsens secondary hyperparathyroidism and may decrease doxercalciferol’s effectiveness in reducing blood iPTH level.

After doxercalciferol therapy starts, expect to decrease dosage of phosphate binders to correct persistent mild hypercalcemia. Expect to increase dosage to correct persistent mild hyperphosphatemia.

Avoid giving magnesium-containing antacids with doxercalciferol if patient receives long-term hemodialysis because doing so may lead to hypermagnesemia.

PATIENT SAFTY

Urge patient who takes doxercalciferol to follow strict low-phosphorus diet and to take calcium supplement, as prescribed, to maintain serum calcium level. Stress that diet and calcium-based phosphate binder should provide 1.5 to 2 g of calcium daily.

Explain importance of periodic follow-up blood work to measure drug effectiveness. Tell the patient that it may take several months to reach optimal PTH suppression.

Warn patient not to take other forms of vitamin D with doxercalciferol and to ask prescriber before taking any OTC drug.

Advise patient to contact prescriber immediately if early signs or symptoms of toxicity, such as headache or nausea, develop.

Category

Chemical class: Oxytetracycline derivative
Therapeutic class: Antibiotic

Pregnancy category: D

Indications

To treat cutaneous, GI, or inhalation anthrax , DELAYED-RELEASE , ORAL SUSPENSION,,
IV: Adults,adolescents,and children weighing more than 45 kg (99 lb). 100 mg (base) every 12 hr for 60 days. Children weighing less than 45 kg. 2.2 mg/ kg (base) every 12 hr for 60 days. To treat inflammatory lesions (papules and pustules) of rosacea
Adults.40 mg once daily in morning To treat endocervical, rectal, and urethral infections caused by Chlamydia trachomatis , DELAYED-RELEASE , ORAL SUSPENSION, Adults and children over age 8 weighing more than 45 kg. 100 mg (base) b.i.d. for 7 days. Maximum: 300 mg (base) daily. Children weighing 45 kg or less. 2.2 mg (base)/kg b.i.d. on day 1 and then 2.2 to 4.4 mg (base)/kg daily or 1.1 to 2.2 mg (base)/kg b.i.d.
IV: Adults and children over age 8 weighing more than 45 kg. 200 mg (base) once daily or 100 mg (base) every 12 hr on day 1 and then 100 to 200 mg (base) once daily or doxycycline 349 D 50 to 100 mg (base) every 12 hr. Maximum: 300 mg (base) daily. Children weighing 45 kg or less. 4.4 mg (base)/kg once daily or 2.2 mg (base)/kg every 12 hr on day 1 and then 2.2 to 4.4 mg (base)/kg once daily or 1.1 to 2.2 mg (base)/kg every 12 hr. To treat epididymo-orchitis caused by C. trachomatis or Neisseria gonorrhoeae or nongonococcal urethritis caused by C. trachomatis or Ureaplasma urealyticum , DELAYED-RELEASE , ORAL SUSPENSION, Adults and children over age 8 weighing more than 45 kg. 100 mg (base) b.i.d. for at least 10 days. Maximum: 300 mg (base)/day. Children weighing 45 kg or less. 2.2 mg (base)/kg b.i.d. on day 1 and then 2.2 to 4.4 mg (base)/kg once daily or 1.1 to 2.2 mg (base)/kg b.i.d.
IV: Adults and children over age 8 weighing more than 45 kg. 200 mg (base) once daily or 100 mg (base) every 12 hr on day 1 and then 100 to 200 mg (base) once daily or 50 to 100 mg (base) every 12 hr. Maximum: 300 mg (base) daily. Children weighing 45 kg or less. 4.4 mg (base)/kg once daily or 2.2 mg (base)/kg every 12 hr on day 1 and then 2.2 to 4.4 mg (base)/kg once daily or 1.1 to 2.2 mg (base)/kg every 12 hr. To prevent malaria , DELAYED-RELEASE , ORAL SUSPENSION, Adults and children over age 8 weighing more than 45 kg. 100 mg (base) daily starting 1 to 2 wk before travel, continued daily during travel, and then daily for 4 wk after travel ends. Maximum: 300 mg (base) daily. Children over age 8. 2 mg (base)/kg daily starting 1 to 2 days before travel, continued daily during travel, and daily for 4 wk after travel ends. Maximum: 100 mg (base) daily. To treat early syphilis in penicillinallergic patients , DELAYED-RELEASE , ORAL SUSPENSION, Adults and children over age 8 weighing more than 45 kg. 100 mg (base) b.i.d. for 2 wk. Maximum: 600 mg (base) daily. Children weighing 45 kg or less. 2.2 mg (base)/kg b.i.d. on day 1 and then 2.2 to 4.4 mg (base)/kg once daily or 1.1 to 2.2 mg (base)/kg b.i.d.
IV: Adults and children over age 8 weighing more than 45 kg. 150 mg (base) every 12 hr for at least 10 days. Maximum: 300 mg (base) daily. Children weighing 45 kg or less. 4.4 mg (base)/kg once daily or 2.2 mg (base)/kg every 12 hr on day 1 and then 2.2 to 4.4 mg (base)/kg once daily or 1.1 to 2.2 mg (base)/kg every 12 hr. To treat syphilis of more than 1 year’s duration in penicillin-allergic patients , DELAYED-RELEASE , ORAL SUSPENSION, Adults and children over age 8 weighing more than 45 kg. 100 mg (base) b.i.d. for 4 wk. Maximum: 300 mg (base) daily.
IV: Adults and children over age 8 weighing more than 45 kg. 150 mg (base) every 12 hr for at least 10 days. Maximum: 300 mg (base) daily. Children weighing 45 kg or less. 4.4 mg (base)/kg once daily or 2.2 mg (base)/kg every 12 hr on day 1 and then 2.2 to 4.4 mg (base)/kg once daily or 1.1 to 2.2 mg (base)/kg every 12 hr. To treat all other infections caused by susceptible organisms , DELAYED-RELEASE , ORAL SUSPENSION, Adults and children over age 8 weighing more than 45 kg. 100 mg (base) every 12 hr on day 1 and then 100 mg (base) once daily or 50 mg (base) b.i.d. For severe infections, 100 mg (base) continued every 12 hr. Maximum: 300 mg (base) daily. Children weighing 45 kg or less. 2.2 mg (base)/kg b.i.d. on day 1 and then 2.2 to 4.4 mg (base)/kg once daily or 1.1 to 2.2 mg (base)/kg b.i.d.
IV: Adults and children over age 8 weighing more than 45 kg. 200 mg (base) once daily or 100 mg (base) every 12 hr on day 1 and then 100 to 200 mg (base) once daily or 50 to 100 mg (base) every 12 hr. Maximum: 300 mg (base) daily. Children weighing 45 kg or less. 4.4 mg (base)/kg once daily or 2.2 mg (base)/kg every 12 hr on day 1 and then 2.2 to 4.4 mg (base)/kg once daily or 1.1 to 2.2 mg (base)/kg every 12 hr. doxycycline 350

Mechanism of Action

Exerts a bacteriostatic effect against a wide variety of gram-positive and gram-negative organisms. Doxycycline is more lipophilic than other tetracyclines, which allows it to pass more easily through the bacterial lipid bilayer, where it binds reversibly to 30S ribosomal subunits. Bound doxycycline blocks the binding of aminoacyl transfer RNA to messenger RNA, thus inhibiting bacterial protein synthesis.

Contraindications

Hypersensitivity to any tetracycline

Interactions

antacids that contain aluminum, calcium, magnesium, or zinc; calcium supplements; choline and magnesium salicylates; iron salts; laxatives that contain magnesium: Decreased doxycycline absorption and effects barbiturates, carbamazepine,
phenytoin: Increased clearance and decreased effects of doxycycline cholestyramine, colestipol: Decreased doxycycline absorption digoxin: Increased bioavailability of digoxin, possibly leading to digitalis toxicity oral anticoagulants: Possibly increased hypoprothrombinemic effects of these oral contraceptives: Decreased effectiveness of estrogen-containing oral contraceptives, increased risk of breakthrough bleeding penicillins: Inhibited bactericidal action penthrane: Possibly increased risk of fatal renal toxicity sodium bicarbonate: Altered doxycycline absorption from increased gastric pH dairy products, other high in calcium or iron: Decreased doxycycline absorption

Side Efect

CNS: Paresthesia
CV: Phlebitis
EENT: Black “hairy”tongue, glossitis, hoarseness, oral candidiasis, pharyngitis, stomatitis, tooth discoloration
GI: Anorexia; bulky, loose stools; diarrhea; dysphagia; enterocolitis; epigastric distress; esophageal ulceration; hepatotoxicity; nausea; pseudomembranous colitis; rectal candidiasis; vomiting
GU: Anogenital lesions, dark yellow or brown urine, elevated BUN level, vaginal candidiasis
HEME: Eosinophilia, hemolytic anemia, neutropenia, thrombocytopenia, thrombocytopenic purpura
SKIN: Dermatitis, photosensitivity, rash, urticaria
Other: Anaphylaxis, injection site phlebitis

Cautions

Avoid giving doxycycline to breastfeeding women because of the risk of enamel hypoplasia, inhibited linear skeletal growth, oral and vaginal candidiasis, photosensitivity reactions, and tooth discoloration in breastfeeding infant.

Avoid giving drug to children under age 8, if possible; it may cause discoloration and enamel hypoplasia of developing teeth.

Use oral suspension cautiously in patients allergic to sulfites because it contains sodium metabisulfite.

Expect to adjust dosage for patients who have hepatic disease to avoid drug accumulation.
WARNING Don’t give doxycycline by I.M. or subcutaneous route.

Give doxycycline without regard to meals. Food and milk may delay absorption, but they don’t significantly reduce it.

Observe patient often for injection site phlebitis, a common adverse reaction to I.V. administration.

Monitor liver function test results as appropriate to detect hepatotoxicity.

Expect oral or parenteral doxycycline to increase risk of oral, rectal, or vaginal candidiasis—especially in elderly or debilitated patients and those on prolonged therapy—by changing the normal balance of microbial flora.

Monitor patient closely for diarrhea, which may indicate pseudomembranous colitis. If diarrhea occurs, notify prescriber and expect to withhold doxycycline. Expect to treat pseudomembranous colitis with fluids, electrolytes, protein, and an antibiotic effective against Clostridium difficile.

PATIENT SAFTY

Instruct patient not to take doxycycline just before bed because it may not dissolve properly when she’s recumbent and may cause esophageal burning and ulceration.

Instruct patient taking doxycycline for rosacea to take the capsule in the morning doxycycline 351 D on an empty stomach.

Advise patient to avoid dairy products; high in calcium or iron; antacids containing aluminum, calcium, or magnesium; bismuth subsalicylate; and ironcontaining products during therapy.

Caution patient not to take bismuth subsalicylate while taking doxycycline because doxycycline absorption will be reduced.

Instruct patient to drink plenty of fluids while taking doxycycline to reduce the risk of esophageal burning and ulceration.

Inform patient that her urine may become dark yellow or brown during therapy.

Urge patient to avoid sun exposure and ultraviolet light as much as possible during therapy and to use sunscreen or sunblock as needed. If patient develops phototoxicity, such as skin eruption, tell her to stop drug and notify prescriber.

Advise patients who take an oral contraceptive to use an additional contraceptive method during therapy.

If patient is being treated for a sexually transmitted disease, explain that her partner may need treatment as well.

Tell patient to notify prescriber immediately about anorexia, epigastric distress, nausea, or vomiting during therapy.

Urge patient to report watery, bloody stools to prescriber immediately, even up to 2 months after drug therapy has ended.

Alert female patients that doxycycline may increase risk of vaginal candidiasis. Tell her to notify prescriber if she develops vaginal itching or discharge.

Advise patient taking doxycycline for malaria prevention to start taking drug 1 to 2 days before traveling to the region and continue for 4 weeks after leaving the area. Note that the total length of therapy shouldn’t exceed 4 months.

Category

Chemical class: Synthetic tetrahydrocannabinol
Therapeutic class: Antiemetic, appetite stimulant

Pregnancy category: C

Controlled substance schedule: II

Indications

To prevent nausea and vomiting caused by chemotherapy and unresponsive to other antiemetics
Adults.5 mg/m21 to 3 hr before and 2 to 4 hr after chemotherapy, increased by 2.5 mg/m2, p.r.n. Maximum: 15 mg/m2/ dose or a total of 4 to 6 doses daily. To stimulate appetite in cancer and AIDS patients
Adults.Initial: 2.5 mg b.i.d. before lunch and supper, increased p.r.n. Maximum: 20 mg daily in divided doses.
DOSAGE ADJUSTMENT Dosage reduced to 2.5 mg before supper or at bedtime for patients who can’t tolerate 5 mg daily. Route Onset Peak Duration P.O. Unknown Unknown 24 hr or longer*

Mechanism of Action

May exert antiemetic effect by inhibiting the vomiting control mechanism in the medulla oblongata. As the main psychoactive substance in marijuana (Cannabis sativa L.), dronabinol’s effects may be mediated by cannabinoid receptors in neural tissues.

Contraindications

Hypersensitivity to dronabinol, its components, sesame oil, or marijuana

Interactions

anticholinergics, antihistamines: Possibly increased risk of tachycardia apomorphine: Possibly potentiated CNS depression, possibly decreased emetic response with prior use of dronabinol CNS stimulants (such as amphetamines), and CNS depressants (such as benzodiazepines): Additive CNS effects sympathomimetics: Possibly enhanced hypertension, tachycardia, and other adverse cardiovascular effects dronabinol 352 * For appetite stimulant effects; unknown for antiemetic effects.
alcohol use: Additive CNS depressant effects

Side Efect

CNS: Amnesia, anxiety, ataxia, confusion, delusions, depression, dizziness, drowsiness, euphoria, fatigue, hallucinations, irritability, mood changes, nervousness, seizures, sleep disturbance
CV: Orthostatic hypotension, palpitations, sinus tachycardia
GI: Nausea, vomiting
Other: Physical and psychological dependence

Cautions

WARNING Dronabinol shouldn’t be discontinued abruptly; if it is, withdrawal syndrome may occur.

Use cautiously in patients with history of seizures because drug may lower seizure threshold. Notify prescriber of seizures immediately, and expect to stop drug.

Patients under age 45 may tolerate drug better than those over age 45.

Watch for

Side Efect

that mimic psychosis, such as hallucinations and, possibly, acute anxiety, especially at high doses.

Anticipate higher risk of cardiovascular reactions, such as increased heart rate and blood pressure changes (especially orthostatic hypotension), at higher doses.
WARNING Expect tolerance to drug to develop over time, especially if patient has smoked marijuana.

Be aware that short-term, low-dose therapy doesn’t typically lead to physical and psychological dependence, which may occur with long-term, high-dose therapy.

Expect drug to alter REM sleep pattern, even after therapy stops.

PATIENT SAFTY

Caution patient not to stop drug abruptly because withdrawal symptoms may occur.

Urge patient not to use alcohol while taking dronabinol because it may enhance CNS depression.

Instruct patient to rise slowly to sitting or standing position to minimize effects of orthostatic hypotension.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Inform patient that sleep pattern may be adversely affected during therapy and for sometime afterward.

Category

Chemical class: Benzofuran derivative
Therapeutic class: Antiarrhythmic

Pregnancy category: X

Indications

To reduce risk of cardiovascular hospitalization in patients with paroxysmal or persistent atrial fibrillation or flutter, with a recent episode of atrial fibrillation or flutter and associated cardiovascular risk factors (i.e., age over 70 years or presence of hypertension, diabetes, prior cerebrovascular accident, left atrial diameter 50 mm or more or left ventricular ejection fraction less than 40%), who are in sinus rhythm or who will be cardioverted
Adults.400 mg twice daily, with morning and evening meals Route Onset Peak Duration P.O. Unknown 3–6 hr Unknown

Mechanism of Action

Although specific effect on heart rhythm is unknown, dronedarone possesses properties of all four Vaughn-Williams antiarrhythmic classes.

Contraindications

Bradycardia less than 50 beats/minute; concurrent use of or herbal products that prolong QT interval, such as class I and III antiarrhythmics, phenothiazine antipsychotics, oral macrolide antibiotics (selected), and tricyclic antidepressants; concurrent use of strong CYP3A inhibitors, such as clarithromycin, cyclosporine, ketoconazole, itraconazole, nefazodone, ritonavir, telithromycin, and voriconazole; hypersensitivity to dronedarone or its components; nursing mothers; NYHA Class IV heart failure or NYHA Class II-III heart failure with a recent decompensation requiring hospitalization or referral to a specialized heart failure clinic; pregnancy; QTc Bazett interval of 500 ms or greater or a PR interval greater than 280 ms; secondor thirddronedarone 353 D degree atrioventricular block or sick sinus syndrome (except when used in with a functioning pacemaker); severe hepatic impairment (Child-Pugh Class C)

Interactions

calcium channel blockers: Possibly increased dronedarone effects on conduction calcium channel blockers, such as diltiazem, nifedipine, and verapamil; CYP3A substrates with narrow therapeutic rang,e such as sirolimus and tacrolimu; CYP2D6 substrates, such as beta blockers, selective serotonin reuptake agents, and tricyclic antidepressant; statins, such as simvastain: Increased effects of these with possibly increased risk of

Side Efect

class I and III antiarrhythmics, macrolide antibiotics, phenothiazinees, tricyclic antidepressants: Possibly increased QT interval CYP3A inducers, such as carbamazepine, phenobarbital, phenytoin, rifampin, St. John’s wort: Decreased dronedarone effects CYP3A inhibitors, such as clarithromycin, cyclosporine, ketoconazole, itraconazole, nefazodone, ritonavir, telithromycin, and voriconazole: Increased dronedarone effects digoxin and other P-gP substrates: Increased effect of these with risk of toxicity; increased risk of adverse GI reactions diltiazem, verapamil: Increased dronedarone effect potassium-depleting diuretics: Increased risk of hypokalemia and hypomagnesemia grapefruit juice: Increased dronedarone effects

Side Efect

CNS: Asthenia
CV: Bradycardia, heart failure, prolonged QT interval
GI: Abdominal pain, diarrhea,dyspepsia, nausea, vomiting
GU: Increased serum creatinine levels
SKIN: Allergic dermatitis, dermatitis, eczema, photosensitivity, pruritus, rash

Cautions

Check that patient has stopped taking any drug contraindicated with dronedarone, as prescribed, before giving first dose.

Monitor patient for evidence of heart failure, such as weight gain, dependent edema, or increasing shortness of breath. If present, notify prescriber; dronedarone may need to be discontinued.

Monitor patient’s PR and QT interval, as ordered, to see if conduction is delayed. If so, notify prescriber immediately. Dronedarone will need to be stopped.

Monitor patient’s serum creatinine levels, as ordered. Elevation may occur rapidly, plateau after 7 days, and usually is reversible after therapy stops. However, if serum creatinine level increases, be aware that this increased value should be used as the patient’s new baseline.

PATIENT SAFTY

Inform patient that dronedarone must be taken with a meal.

Warn patient that dronedarone should not be taken with grapefruit juice.

Urge patient to contact prescriber if he develops evidence of heart failure, such as weight gain, dependent edema, or increasing shortness of breath, because dronedarone may need to be discontinued.

Inform women of childbearing age of need for contraception if sexually active because drug is contraindicated during pregnancy and breastfeeding. If pregnancy occurs, she should notify prescriber immediately.

Tell patient to inform all prescribers that he is taking dronedarone and to check with prescriber before taking any newly prescribed drug, OTC product, or herbal product with dronedarone.

Category

Chemical class: Butyrophenone derivative
Therapeutic class: Antiemetic

Pregnancy category: C

Indications

To reduce nausea and vomiting after surgery or diagnostic procedures when other treatments are ineffective I.V. OR

IM

Adults and adolescents.Dosage individualized up to a maximum initial dose of 2.5 mg I.M. or slow I.V. Additional 1.25 mg may be given to achieve desired effect if potential benefit outweighs risk. Children ages 2 to 12. Dosage individualdroperidol 354 ized to a maximum initial dose of 0.1 mg/ kg. Additional dose may be given to achieve desired effect if potential benefit outweighs risk.
DOSAGE ADJUSTMENT Initial dosage reduced for elderly, debilitated, or critically ill patients because of the increased risk of hypotension and excessive sedation. Route Onset Peak Duration I.V., I.M. 3–10 min In 30 min 2–4 hr

Mechanism of Action

Produces sedation by blocking postsynaptic dopamine receptors in limbic system. Droperidol may reduce nausea by blocking dopamine receptors in chemoreceptor trigger zone in reticular formation of the medulla oblongata. It also may produce antiemetic effects by attaching to postsynaptic gamma-amino-butyric acid (GABA) receptors in the chemoreceptor trigger zone.

Contraindications

Hypersensitivity to droperidol or its components, known or suspected prolonged QT interval (including congenital long-QT syndrome)

Interactions

amoxapine, haloperidol, loxapine, metoclopramide, metyrosine, molindone, olanzapine, phenothiazines, pimozide, rauwolfia alkaloids, risperidone, tacrine,
thioxanthenes: Possibly increased risk of severe extrapyramidal reactions anesthetics: Possibly hypotension and peripheral vasodilation antiarrhythmics (class I or III), antidepressants, antimalarials, benzodiazepines, diuretics, I.V. opioids, laxatives, MAO inhibitors, volatile anesthetics, and other that prolong QT interval (such as some antihistamines): Increased risk of serious adverse effects of droperidol, such as prolonged QT interval and arrhythmias antihypertensives: Possibly orthostatic hypotension bromocriptine, levodopa: Possibly inhibited actions of these
CNS depressants: Additive CNS depression epinephrine: Possibly paradoxical reduction of blood pressure propofol: Possibly decreased antiemetic effect of both
alcohol use: Additive CNS depression

Side Efect

CNS: Anxiety, drowsiness, dystonia, restlessness
CV: Cardiac arrest, hypertension, hypotension, potentially fatal arrhythmias (such as torsades de pointes and ventricular tachycardia), prolonged QT interval, sinus tachycardia
EENT: Fixed upward position of eyeballs, laryngospasm
MS: Spasms of tongue, face, neck, and back muscles
RESP: Bronchospasm

Cautions

WARNING Use droperidol cautiously in patients over age 65 and in patients with alcoholism, bradycardia, heart failure, hypokalemia, hypomagnesemia, parkinsonism, or preexisting QT-interval prolongation because they’re at increased risk for prolonged QT interval and potentially fatal

Side Efect

. Patients who take that prolong the QT interval, such as some antiarrhythmics and benzodiazepines, and patients who take that may cause an electrolyte imbalance, such as diuretics and laxatives, are also at increased risk.

Expect a 12-lead ECG to be performed on all patients before droperidol administration to verify the absence of prolonged QT interval. Monitor ECG continuously for 2 to 3 hours after administering drug. Also monitor serum electrolyte levels to detect electrolyte imbalances.

Use droperidol cautiously in patients with cardiac disease, who may not be able to compensate for drug’s hypotensive effect. Monitor vital signs, including blood pressure, frequently. Be aware that hypertension and tachycardia may occur in patients with a history of pheochromocytoma.

Expect altered level of consciousness to last up to 12 hours after drug is given. Expect dosage to be reduced if patient is taking an opioid analgesic.

If drug causes extrapyramidal reactions, such as restlessness, dystonia, and oculogyric crisis, expect to administer an antidroperidol 355 D cholinergic, such as benztropine or diphenhydramine. Be sure to maintain a patent airway and oxygenation.

If patient develops severe hypotension, expect to give phenylephrine. If hypotension is related to hypovolemia, expect to administer fluids.

PATIENT SAFTY

Advise patient to immediately report palpitations or faintness, which may indicate an abnormal cardiac rhythm.

Instruct patient to ask for help with ambulation on first postoperative day because altered consciousness may last up to 12 hours.

Caution patient to avoid drinking alcohol, taking CNS depressants, driving, and operating machinery for 24 hours after receiving droperidol.

Category

Chemical class: Serine protease glycoprotein
Therapeutic class: Anti-inflammatory, antithrombolytic

Pregnancy category: C

Indications

To reduce risk of death in patients with severe sepsis in acute organ dysfunction

IV

Adults. 24 mcg/kg/hr for 96 hr.

Mechanism of Action

Interferes with a number of body responses to severe sepsis, including increased thrombin generation and fibrin formation, impaired fibrinolysis, and systemic inflammation. Drotrecogin alfa produces antithrombotic effect by inhibiting factors Va and VIIIa and indirect profibrinolytic effect by inhibiting plasminogen activator inhibitor-1 and limiting generation of activated thrombin-activatable fibrinolysis inhibitor. Drotrecogin may produce antiinflammatory effect by inhibiting production of human tumor necrosis factor and other cytokines, preventing leukocyte adhesion to selectins, and limiting thrombininduced inflammatory responses in the microvascular endothelium.

Incompatibilities

Don’t infuse any or solutions except D5W, normal saline solution, lactated Ringer’s solution, or dextrose and saline mixtures through drotrecogin alfa I.V. line.

Contraindications

Active internal bleeding; evidence of cerebral herniation; hemorrhagic stroke in the past 3 months; hypersensitivity to drotrecogin alfa or its components; intracranial or intraspinal surgery or severe head trauma in the past 2 months; intracranial neoplasm or lesion; presence of epidural catheter; trauma with an increased risk of lifethreatening bleeding

Interactions

abciximab, eptifibatide, and other glycoprotein IIb/IIIa inhibitors; aspirin and other platelet inhibitors; heparin; oral anticoagulants; thrombolytics: Increased risk of bleeding

Side Efect

CNS: Intracranial hemorrhage
CV: Intrathoracic bleeding
GI: GI, intra-abdominal, or retroperitoneal bleeding
GU: Genitourinary bleeding
HEME: Prolonged APTT
SKIN: Ecchymosis

Cautions

Be aware that drotrecogin alfa is used only for patients with severe sepsis who are at high risk for death, as determined by an Acute Physiology and Chronic Health Evaluation (APACHE) II score, a method of assessing mortality risk. Patients with only single-organ dysfunction who are recovering from recent surgery may not be candidates for drotrecogin alfa despite an adequate APACHE II score.

Reconstitute 5-mg and 20-mg vials by slowly adding 2.5 ml or 10 ml sterile water for injection, respectively, to yield 2 mg/ ml. Gently swirl—don’t shake—vial until powder is completely dissolved. Use drotrecogin alfa 356 immediately or store for up to 3 hours at 59° to 86° F (15° to 30° C).

Add reconstituted drug to normal saline solution by directing stream to side of bag to minimize agitation. Gently invert bag to mix; don’t shake. Dilute to final concentration of 100 to 200 mg/ml if drug will be given by I.V. infusion pump or 100 to 1,000 mg/ml if by syringe pump. Infusion bag should not be transported by a mechanical delivery system, such as a tube delivery system, between pharmacy and nursing unit.

Prime infusion set for 15 minutes at a flow rate of 5 ml/hour when infusing less than 200 mg/ml at less than 5 ml/hour. Use prepared I.V. solution within 12 hours.

Give drotrecogin alfa through a dedicated I.V. line or lumen of a multilumen central venous catheter. Don’t infuse any or solutions except D5W, normal saline solution, lactated Ringer’s solution, or dextrose and saline mixtures through the same line.

Be aware that total duration of the drotrecogin alfa infusion must equal 96 hours, even if you need to interrupt it for a period. For example, if you calculate that infusion should end on 5 p.m. Friday, but then have to stop to give the patient blood for 2 hours on Thursday, add those 2 hours to your estimated completion time, which would then be 7 p.m. Friday.
WARNING Monitor patient closely for bleeding; if it occurs, stop drotrecogin alfa infusion immediately and notify prescriber. Patients at increased risk include those with chronic severe hepatic disease, intracranial arteriovenous malformation or aneurysm, known bleeding diathesis, GI bleeding in previous 6 weeks, or ischemic stroke in previous 3 months; those receiving concurrent therapeutic heparin (15 units/kg/hour or more); those who have received thrombolytic therapy in previous 3 days, aspirin at more than 650 mg daily, other platelet inhibitors in previous 7 days, or oral anticoagulants or glycoprotein IIb/IIIa inhibitors in previous 7 days; those with any other condition in which bleeding would constitute a significant hazard or be difficult to manage because of its location; and those with a platelet count less than 30,000 3 106/L or PT (as INR) greater than 3.0.

Expect to discontinue drotrecogin alfa 2 hours before an invasive surgical or other procedure that poses a risk of bleeding and to resume administration immediately after uncomplicated, less-invasive procedures or 12 hours after major invasive procedures or surgery at the same rate of 24 mg/kg/hour, as prescribed.

Be aware that drotrecogin alfa may prolong APTT during administration; PT may need to be used to monitor coagulopathy status during treatment.

Before using drotrecogin alfa, refrigerate it at 36° to 46° F (2° to 8° C); don’t freeze it. Protect from heat and direct sunlight.

PATIENT SAFTY

Teach patient about

Side Efect

to drotrecogin alfa, including bleeding from gums or nose and increased bruising. Instruct her to immediately report any signs of bleeding.

Reassure patient that she’ll be monitored closely throughout therapy.

Category

Chemical: Selective serotonin and norepinephrine reuptake inhibitor Therapeutic: Antidepressant, neuropathic pain reliever

Pregnancy category: C

Indications

To treat major depressive disorder
Adults.20 mg b.i.d. Alternatively, 60 mg once daily or 30 mg b.i.d. To relieve neuropathic pain associated with diabetic peripheral neuropathy
Adults. 60 mg daily. To treat generalized anxiety disorder
Adults. Initial: 30 or 60 mg once daily, increased in 30-mg increments weekly, as needed. Maximum: 120 mg once daily. To treat fibromyalgia
Adults. Initial: 30 mg daily for 1 wk; then duloxetine hydrochloride 357 D increased to 60 mg daily.

Mechanism of Action

Inhibits neuronal serotonin, norepinephrine, and dopamine reuptake to potentiate serotonergic and noradrenergic activity in the CNS. These activities may elevate mood and inhibit pain signals stemming from peripheral nerves adversely affected by chronically elevated serum glucose level. Route Onset Peak Duration P.O. Unknown 6 hr Unknown

Contraindications

Hepatic insufficiency, hypersensitivity to duloxetine or its components, uncontrolled angle-closure glaucoma, use within 14 days of MAO inhibitor therapy

Interactions

amiodarone, celecoxib, cimetidine, erythromycin, fluoxetine, fluvoxamine, haloperidol, ketoconazole, methadone, paroxetine, quinidine, quinolones, ritonavir: Increased blood duloxetine level amiodarone, amitriptyline, desipramine, flecainide, haloperidol, imipramine, methadone, nortriptyline, phenothiazines, propafenone, ritonavir, thioridazine: Increased blood levels of these aspirin, NSAIDs,
warfarin: Possibly increased risk of bleeding CNS : Increased effect of duloxetine
MAO inhibitors: Serious, sometimes fatal, autonomic instability, hyperthermia, myoclonus, rigidity plasma protein binders (warfarin, phenytoin): Increased free concentration of these and increased risk of adverse reactions serotonergic : Increased risk of serotonin syndrome
alcohol use: Increased risk of hepatotoxicity

Side Efect

CNS: Abnormal dreams, aggression, agitation, anger, anxiety, asthenia, chills, dizziness, extrapyramidal disorder, fatigue, fever, hallucinations, headache, insomnia, migraine, nervousness, neuroleptic malignant syndrome, parasthesia, restless legs syndrome, serotonin syndrome, somnolence, suicidal ideation, syncope, tremor, vertigo
CV: Hypertension, hypertensive crisis, orthostatic hypotension, palpitations, paresthesia, peripheral edema, supraventricular arrhythmia
EENT: Blurred vision, dry mouth, glaucoma, nasopharyngitis, pharyngitis, taste alteration
ENDO: Hot flashes, hyperglycemia
GI: Abdominal pain, anorexia, cholestatic jaundice, constipation, diarrhea, elevated liver enzymes, flatulence, hepatitis, hepatotoxicity, indigestion, jaundice, nausea, upper abdominal pain, vomiting
GU: Abnormal orgasm, decreased libido, erectile or ejaculatory dysfunction, urinary frequency, UTI
HEME: Bleeding episodes, leukopenia, thrombocytopenia
MS: Arthralgia, back pain, extremity pain, muscle cramp, myalgia
RESP: Cough, upper respiratory tract infection
SKIN: Diaphoresis, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome, urticaria
Other: Anaphylaxis, angioedema, hyponatremia, weight loss

Cautions

Avoid giving duloxetine to patients with severe renal impairment or end-stage renal disease that requires hemodialysis because blood drug levels increase significantly in these patients. Also avoid duloxetine in patients with hepatic insufficiency because drug is metabolized by the liver.

Use duloxetine cautiously in patients with delayed gastric emptying because drug’s enteric coating resists dissolution until it reaches an area where pH exceeds 5.5.

Give duloxetine cautiously to patients with a history of mania, which it may activate. Also give cautiously to patients with a seizure disorder because drug effects aren’t known in these patients.

Obtain patient’s baseline blood pressure before duloxetine therapy starts, and assess it periodically thereafter for changes. If orthostatic hypotension occurs during therapy, notify prescriber and anticipate that drug may need to be discontinued.

Monitor patient’s serum sodium level, especially if patient is elderly, is taking a duloxetine hydrochloride 358 diuretic, or has volume depletion, because drug may lower serum sodium level.

Monitor patient’s hepatic function, as ordered, because drug may increase the risk of hepatotoxicity.

If patient takes duloxetine for depression (especially if he’s a child or an adolescent), watch closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

Avoid stopping duloxetine therapy abruptly, if possible, because withdrawal symptoms such as dizziness, nausea, headacle, fatigue, paresthesia, vomiting, irritability, nightmares, insomnia, diarrhea, anxiety, hyperhidrosis, and vertigo may occur. Taper dosage gradually, as ordered.
WARNING Monitor patient for serotonin syndrome, characterized by agitation, chills, confusion, diaphoresis, diarrhea, fever, hyperactive reflexes, poor coordination, restlessness, shaking, talking or acting with uncontrolled excitement, tremor, and twitching. In its most severe form, serotonin syndrome can resemble neuroleptic malignant syndrome, which includes a high fever, muscle rigidity, autonomic instability with possible fluctuations in vital signs, and mental status changes.

PATIENT SAFTY

Tell patient to take capsule whole and not to chew it, crush it, or sprinkle contents on food or liquids because doing so alters enteric coating and may affect drug absorption.

Inform patient that full effect of duloxetine may take weeks to occur; stress the importance of continuing to take the drug as directed.

Caution patient against excessive alcohol consumption while taking duloxetine because it may increase risk of hepatic dysfunction.

Advise patient not to stop duloxetine abruptly because

Side Efect

may occur. Explain that drug will be stopped gradually.

Instruct patient to notify prescriber if any serious or troublesome adverse effects develop.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to rise from a lying or sitting position slowly to minimize drug’s effect on lowering blood pressure.

If patient takes duloxetine for depression, urge caregivers to watch closely for evidence of suicidal tendencies, especially if patient is a child or an adolescent and especially when therapy starts or dosage changes.

Instruct female patients of childbearing potential to notify prescriber if they are, could be, or wish to become pregnant; duloxetine therapy may cause adverse reactions in neonates exposed to it during the third trimester.

Category

Chemical class: Synthetic 4-azasteroid compound
Therapeutic class: Benign prostatic hyperplasia agent

Pregnancy category: X

Indications

To treat symptomatic benign prostatic hyperplasia (BPH); as adjunct with tamsulosin therapy to treat symptomatic BPH Adult men.0.5 mg daily.

Contraindications

Children; women; hypersensitivity to dutasteride, its components, or other 5-alpha reductase inhibitors

Interactions

cimetidine, ciprofloxacin, diltiazem, ketoconazole, ritonavir, verapamil, and other CYP3A4 inhibitors: Risk of decreased dutasteride metabolism and enhanced effects

Side Efect

CNS: Dizziness
ENDO: Gynecomastia, increased serum testosterone and thyroid-stimulating hormone levels
GU: Decreased ejaculatory volume, decreased libido, impotence
SKIN: Localized edema, pruritus, rash, serious skin reactions, urticaria
ENDO: Angioedema dutasteride 359 D

Cautions

WARNING Be aware that dutasteride is absorbed through the skin. If you are female and pregnant or of childbearing age, do not handle dutasteride capsule when administering it to a patient.

Patient should be evaluated for other urologic conditions, including prostate cancer, before dutasteride therapy starts.

Expect patient to undergo a digital rectal examination of the prostate before and periodically during dutasteride therapy.

Anticipate need to obtain a new baseline prostate-specific antigen (PSA) value after 3 to 6 months of dutasteride treatment because drug can decrease PSA concentration by 40% to 50%.

PATIENT SAFTY

WARNING Urge patient and female partners to use reliable contraceptive method during dutasteride therapy because semen of men who take drug can harm male fetuses. Caution women and children against handling capsules.

Advise patient to inform prescriber if he has liver disease.

Explain how to take drug properly, and advise patient to follow instructions that accompany drug. Instruct him to swallow capsule whole and to notify pharmacist if capsules are cracked or leaking.

Inform patient that drug may decrease ejaculatory volume and libido and may cause impotence.

Instruct patient to postpone blood donations for 6 months after final dose to avoid transmitting dutasteride to a pregnant woman during a blood transfusion.

Urge patient to have periodic follow-up appointments.

Category

Chemical class: Xanthine derivative dyphylline 360 DHT Testosterone Dutasteride Cell Blood vessel 5α-R DHT DHT DHT Testosterone Dutasteride Cell Blood vessel 5α-R DHT DHT

Mechanism of Action

Dutasteride reduces prostate gland enlargement by inhibiting conversion of testosterone to its active metabolite, 5-alpha dihydrotestosterone (DHT). DHT is the main hormone that stimulates prostate cells to grow. As men age, they may become more sensitive to DHT, resulting in excessive growth of prostatic cells and enlargement of the prostate. This condition, benign prostatic hyperplasia, may cause urinary hesitancy, urinary urgency, and nocturia. Two forms of the intracellular enzyme 5alpha-reductase (5a-R types 1 and 2) in liver, prostate, and skin, convert testosterone to DHT, as shown below left. Dutasteride, a dual 5a-R inhibitor, deactivates both forms. When 5a-R is inhibited by dutasteride, production of DHT is suppressed, as shown below right. With less circulating DHT, the prostate gland shrinks and symptoms improve.
Therapeutic class: Bronchodilator

Pregnancy category: C

Indications

To prevent or relieve bronchospasm from acute and chronic bronchial asthma, chronic bronchitis, and emphysema ELIXIR,
Adults. Up to 15 mg/kg every 6 hr.
I.M.INJECTION
Adults.Initial: 500 mg. Maintenance: 250 to 500 mg every 2 to 6 hr, as needed.

Mechanism of Action

May cause bronchodilation by inhibiting phosphodiesterase enzymes. These enzymes normally inactivate cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), which are responsible for bronchial smooth-muscle relaxation. Drug also may foster calcium translocation, prostaglandin antagonism, catecholamine stimulation, and adenosinereceptor antagonism.

Contraindications

Hypersensitivity to dyphylline, xanthines, or their components; peptic ulcer disease; seizure disorder (unless controlled by anticonvulsant therapy)

Interactions

beta blockers: Possibly inhibited bronchodilation by dyphylline ephedrine: Possibly increased frequency of insomnia, nausea, and nervousness hydrocarbon inhalation anesthetics: Possibly increased risk of ventricular arrhythmias probenecid: Possibly decreased renal excretion of dyphylline sucralfate: Possibly adsorption of dyphylline if given within 2 hours of each other

Side Efect

CNS: Headache, insomnia, irritability, nervousness, seizures, tremor
CV: Arrhythmias, hypotension, tachycardia
GI: Diarrhea, gastroesophageal reflux, nausea, vomiting
GU: Increased diuresis

Cautions

Inspect I.M. form of dyphylline for precipitate. If present, discard drug and obtain a new ampule.

Give oral drug at least 1 hour after meals for best absorption. However, if drug causes GI distress, give it with food if prescribed.

Don’t give parenteral drug by I.V. route.

Evaluate for therapeutic response, including decreased respiratory rate and effort.

Assess for signs of dyphylline toxicity, including seizures and ventricular tachycardia. PATIENT TTEACHING

Instruct patient to take oral dyphylline with a full glass of water and on an empty stomach to promote absorption.

Advise patient to consult prescriber about taking drug with food if she experiences GI distress.

Category

Chemical class: 60-amino-acid protein
Therapeutic class: Kallikrein inhibitor replacement

Pregnancy category: C

Indications

To treat acute attacks of hereditary angioedema in patients age 16 and older SUBCUTANEOUS INJECTION
Adults. 30 mg (3 ml) given in divided doses of 10 mg (1 ml) each and repeated, if needed, within 24 hr. Route Onset Peak Duration P.O. 24–50 min 2–3 hr Unknown

Mechanism of Action

Blocks conversion of kininogen to bradykinin by binding to plasma kallikrein. Without bradykinin, the inflammatory pathway is not initiated and signs and symptoms of angioedema are relieved. The kallikrein-kinin system is a complex proteolytic cascade that initiates the inflammatory and coagulation pathways through conversion of kininogen to bradykinin by kallikrein. In hereditary angioedema, normal regulation of plasma kallikrein activity and the classical complement cascade is not present because of the absence of a kallikrein inhibitor. This allows kininogen to be converted to bradykinin unchecked, resulting in an excessive amount of bradykinin circulating in plasma. Bradykinin is a vasodilator that may be responsible for the symptoms of hereditary angioedema such as swelling, inflammation, and pain.

Contraindications

Hypersensitivity to ecallantide or its components

Side Efect

CNS: Fatigue, fever, headache
EENT: Nasopharyngitis
GI: Diarrhea, nausea, upper abdominal pain, vomiting
RESP: Upper respiratory infection
SKIN: Pruritus
Other: Anaphylaxis; antibody formation to ecallantide; injection site reactions such as bruising, erythema, irritation, pain, pruritus, and uriticaria

Cautions

Ecallantide must be administered in a setting equipped to treat life-threatening hypersensitivity reactions.

Refrigerate ecallantide and protect from light until time of administration.

Using aseptic technique, withdraw 1 ml (10 mg) from 10-mg vial using a largebore needle. Then, change needle on the syringe to a 27G subcutaneous needle. Repeat procedure for remaining two vials in dose pack.

Give three injections of ecallantide subcutaneously into skin of abdomen, thigh, or upper arm. The injections may be in the same or different anatomic locations because there is no need for site rotation. However, the sites should be separated from each other by at least 5 cm (2 in). Also, don’t use any site where signs and symptoms of the attack are located.
WARNING Monitor patient closely for hypersensitivity reactions, including anaphylaxis, especially within 1 hour of administration. Signs and symptoms may be similar to those of a hereditary angioedema attack. Immediately report chest pain, flushing, pharyngeal edema, pruritus, rhinorrhea, sneezing, nasal congestion, throat irritation, urticaria, wheezing, and hypotension, and be prepared to provide emergency supportive care, as ordered.

PATIENT SAFTY

Explain that a dose requires three injections and that it may be repeated within 24 hours if needed.

Stress importance of reporting any unusual signs and symptoms immediately after receiving ecallantide, such as wheezing, shortness of breath, cough, chest tightness, trouble breathing, dizziness, fainting, fast or weak heartbeat, nervousness, swelling of throat or tongue, throat tightness, hoarse voice, trouble swallowing, runny nose or sneezing, reddening of face, itching, hives or feeling warm.

Category

Chemical class: Difluoromethylornithine
Therapeutic class: Antiprotozoal

Pregnancy category: C

Indications

To treat the meningoencephalitic stage of Trypanosoma brucei gambiense infection (sleeping sickness)

IV

Adults.100 mg/kg given over at least 45 min every 6 hr for 14 days. Route Onset Peak Duration I.V. Unknown 4–6 hr Unknown

Mechanism of Action

Inhibits the enzyme ornithine decarboxylase, which is needed for decarboxylation of ornithine. This process is the first step in polyamine synthesis, which is needed for protozoal cell division and differentiation.

Incompatibilities

Don’t give eflornithine with any other drug.

Contraindications

Hypersensitivity to eflornithine or its components

Side Efect

CNS: Asthenia, dizziness, headache, seizures
EENT: Hearing loss
GI: Abdominal pain, anorexia, diarrhea, vomiting
HEME: Anemia, eosinophilia, leukopenia, myelosuppression, thrombocytopenia
Other: Alopecia, facial edema

Cautions

Plan to reduce eflornithine dosage as prescribed, based on renal function. Monitor creatinine clearance in patients with renal dysfunction.

Before infusion, dilute eflornithine concentrate with sterile water for injection. Using strict aseptic technique, withdraw the contents of a 100-ml vial and inject 25 ml into each of four I.V. diluent bags that contain 100 ml of sterile water. The resulting solution contains 40 mg/ml of eflornithine (5,000 mg of eflornithine in 125 ml total volume).

Store bags of diluted eflornithine at 4° C (39° F) to reduce the risk of contamination. Use diluted drug within 24 hours.

Expect to monitor the patient’s CBC, including platelet count, before eflornithine treatment, twice weekly during treatment, and weekly after treatment stops until the patient’s hematologic values return to baseline.

Take infection-control and bleeding precautions because drug may cause myelosuppression. Adjust dosage or stop therapy as prescribed, based on severity.

Take seizure precautions during eflornithine therapy.

Consult prescriber about the need for serial audiography, if appropriate.

Store undiluted vials of eflornithine at room temperature, and protect from freezing and light.

PATIENT SAFTY

Stress need for follow-up visits because risk of relapse lasts 24 months after treatment.

Teach patient how to follow infectioncontrol and bleeding precautions if myelosuppression occurs.

Warn patient about risk of seizures; advise against performing potentially hazardous activities during therapy.

Category

Chemical class: Serotonin 5-HT1D–receptor agonist
Therapeutic class: Antimigraine agent

Pregnancy category: C

Indications

To relieve acute migraine attacks with or without aura
Adults.Initial: 20 or 40 mg as a single dose. Repeated in 2 hr, as needed and ordered. eflornithine hydrochloride;eletriptan hydrobromide 364 Maximum: 40 mg as single dose, 80 mg daily.

Mechanism of Action

May stimulate 5-HT1receptors, causing selective vasoconstriction of inflamed and dilated cranial blood vessels in carotid circulation, which decreases carotid arterial blood flow and relieves acute migraines.

Contraindications

Bibasilar or hemiplegic migraine, cardiovascular disease (significant), cerebrovascular syndromes (stroke, transient ischemic attack), hepatic impairment (severe), hypersensitivity to eletriptan or components, ischemic bowel disease, ischemic or vasospastic coronary artery disease (CAD), peripheral vascular disease, uncontrolled hypertension, use within 24 hours of another serotonin 5-HT1–receptor agonist or ergot-type drug, use within 72 hours of a potent CYP3A4 inhibitor

Interactions

clarithromycin, ketoconazole, itraconazole, nefazodone, nelfinavir, ritonavir, troleandomycin and other potent CYP3A4 inhibitors: Increased metabolism of eletriptan and decreased blood eletriptan level ergot-containing , 5-HT1-receptor agonists: Possibly additive or prolonged vasoconstrictive effects fluoxetine, fluvoxamine, paroxetine, sertraline: Increased risk of weakness, hyperreflexia, and incoordination

Side Efect

CNS: Asthenia, dizziness, headache, paresthesia, somnolence, tiredness, weakness
CV: Chest tightness, pain, or pressure; coronary artery vasospasm; hypertension, MI or myocardial ischemia (transient); ventricular fibrillation or tachycardia
EENT: Dry mouth, throat tightness
GI: Abdominal pain, cramps, discomfort, or pressure; dysphagia; indigestion; nausea
SKIN: Flushing
Other: Feeling of warmth, pain, or pressure

Cautions

Ensure that patients who are at risk for CAD undergo a satisfactory CV evaluation before you administer the first dose of eletriptan and that they have a periodic reevaluation of their cardiac status during intermittent long-term therapy.

Obtain an ECG immediately after first dose of drug in patients who have CV risk factors but who have had a satisfactory CV evaluation because of the drug’s potential to cause coronary vasospasm.

Evaluate patient for CV signs and symptoms after administration of eletriptan and notify prescriber if they occur. Expect drug to be withheld, as ordered, while patient undergoes an extensive CV workup, and discontinued if abnormalities are detected.

Monitor patient’s blood pressure during therapy because of drug’s potential to increase blood pressure.

PATIENT SAFTY

Advise patient to take eletriptan as soon as possible after onset of migraine symptoms.

Urge patient to contact prescriber and avoid taking drug if headache symptoms aren’t typical.

Advise against exceeding prescribed dose.

Instruct patient to seek emergency care for chest, jaw, or neck tightness after taking drug because these may indicate adverse CV reactions; subsequent doses may require ECG monitoring.

Urge patient to report palpitations.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Advise yearly ophthalmic examinations during prolonged eletriptan therapy.

Instruct patient to inform prescriber of all he’s taking, including OTC products and herbal remedies.

Category

Chemical class: Biphenyl hydrazone
Therapeutic class: Platelet formation inducer

Pregnancy category: C

Indications

To treat thrombocytopenia in patients with chronic immune (idiopathic) thrombocytopenic purpura and an insufficient response to corticosteroids, eltrombopag olamine 365 E F immunoglobulins, or splenectomy
Adults.Initial: 50 mg daily, increased as needed to maintain a platelet count of 50 3 109/L. Platelet counts usually increase in 1 to 2 wk. Maximum: 75 mg daily.
DOSAGE ADJUSTMENT For patients of East Asian ancestry or patients with moderate to severe hepatic impairment, starting dose of 25 mg daily. Route Onset Peak Duration P.O. Unknown 2–6 hr Unknown

Mechanism of Action

Interacts with the transmembrane domain of the thrombopoietin receptor to signal cascades that induce proliferation and differentiation of megakaryocytes from bone marrow progenitor cells. This action increases platelet production, which is abnormally low in patients with thrombocytopenic purpura.

Contraindications

Hypersensitivity to eltrombopag or its components

Interactions

acetaminophen, atorvastatin, benzylpenicillin, fluvastatin, methotrexate, nateglinide, NSAIDs, opioids, pravastatin, repaglinide, rifampin, rosuvastatin: Possibly increased risk of

Side Efect

related to excessive exposure to these antacids and mineral supplements containing aluminum, calcium, iron, magnesium, selenium, or zinc: Decreased eltrombopag absorption ciprofloxacin, fluvoxamine, gemfibrozil, omep-razole, rifampin, trimethoprim: Increased risk of eltrombopag-induced

Side Efect

all , especially dairy: Decreased absorption of eltrombopag smoking: Increased risk of eltrombopaginduced

Side Efect

and possibly decreased eltrombopag efficacy

Side Efect

CNS: Headache, paresthesia
EENT: Cataract, conjunctival hemorrhage
GI: Abdominal pain, dyspepsia, elevated liver enzymes, hepatotoxicity, nausea, vomiting
GU: Menorrhagia
HEME: Hemorrhage, thrombocytopenia
MS: Fatigue, myalgia
SKIN: Ecchymosis

Cautions

Eltrombopag should be used only to treat chronic immune (idiopathic) thrombocytopenia purpura and not any other kind of thrombocytopenia because of the risk of hematologic malignances.

Eltrombopag can be used only through a restricted distribution program called, Promacta Cares. Patient, pharmacy, and prescriber must all be enrolled before therapy begins.

Use cautiously in patients with hepatic impairment because drug may cause hepatotoxicity.

Monitor liver enzymes and bilirubin level, as ordered, before starting eltrombopag, every 2 weeks during
DOSAGE ADJUSTMENT, and monthly once dose is stable. If abnormalities occur, repeat testing within 3 to 5 days and then weekly until liver enzymes return to baseline. Expect to discontinue drug if alanine aminothransferase level increases to three or more times the upper normal limit, progresses or persists for 4 or more weeks, or is accompanied by an increase in direct bilirubin or clinical symptoms of liver injury.

Obtain baseline CBC, including platelet count and peripheral blood smears, before starting eltrombopag therapy, weekly until stable, and monthly thereafter, as ordered, because thrombopoietin receptor agonists (the same class as eltrombopag) have caused bone marrow fibrosis.

Patient should have a baseline eye examination, as ordered, before starting eltrombopag and periodically throughout therapy, because drug may cause cataracts.

DOSAGE ADJUSTMENTs are based on platelet count response and are not used to normalize platelet counts in order to prevent or minimize thrombotic complications.

Give eltrombopag 1 hour before or 2 hours after the patient has eaten. Separate doses of other by at least 4 hours to prevent drug interactions.

Do not administer more than one dose of eltrombopag olamine 366 eltrombopag within any 24-hour period.

Expect to discontinue drug if improvement doesn’t occur within 4 weeks at maximum dose of 75 mg daily.

Monitor patient for hematologic malignancies because eltrombopag stimulates thrombopoietin receptor on the surface of hematopoietic cells, which increases risk of malignancies.

Monitor patient for increased bleeding after stopping eltrombopag because thrombocytopenia may worsen, increasing bleeding risk, especially if patient is on anticoagulants or antiplatelet therapy. If bleeding occurs, obtain weekly CBC, including platelet count, for at least 4 weeks after therapy stops, and provide supportive care, as indicated and ordered.

PATIENT SAFTY

Inform patient that, before eltrombopag therapy can begin, he must be enrolled in the Promacta Cares program, which provides comprehensive education about the drug.

Urge patient to tell prescriber about all health conditions and all prescribed , OTC , herbs, and supplements taken.

Instruct patient to take eltrombopag on an empty stomach with a full glass of water 1 hour before or 2 hours after a meal and to separate use of other by at least 4 hours because food and certain (such as antacids and iron and vitamin supplements) may interfere with eltrombopag absorption.

Instruct patient to take drug at the same time every day because no more than one dose should be taken within any 24-hour period.

Urge patient to report any adverse reactions to prescriber and to keep all appointments for blood work and follow-up.

Category

Chemical class: Dicarbocyl-containing ACE inhibitor
Therapeutic class: Antihypertensive

Pregnancy category: C

(first trimester), D (later trimesters)

Indications

To control hypertension
Adults.Initial: 5 mg daily, increased after 1 to 2 wk, as needed. Maintenance: 10 to 40 mg once daily or in divided doses b.i.d. Children.0.08 mg/kg daily, titrated according to blood pressure response up to 5 mg daily. Maximum: 0.58 mg/kg/dose or 40 mg/dose.
I.V.INJECTION
Adults.1.25 mg every 6 hr.
DOSAGE ADJUSTMENT Initial dose 2.5 mg P.O. or 0.625 mg I.V. for patients who have sodium and water depletion from diuretic therapy, are receiving diuretics, or have a creatinine clearance below 30 ml/min/ 1.73 m2. If response to I.V. dose is inadequate after 1 hr, I.V. dose of 0.625 mg is repeated and therapy continued at 1.25 mg every 6 hr. To treat heart failure
Adults. Initial: 2.5 mg once or twice daily, increased after 1 to 2 wk, as needed. Maintenance: 5 to 40 mg once daily or in divided doses b.i.d. To treat asymptomatic left ventricular dysfunction
Adults. Initial: 2.5 mg b.i.d., increased to 20 mg daily in divided doses.
DOSAGE ADJUSTMENT Initial dosage reduced to 2.5 mg daily and, if possible, diuretic dosage reduced in patients who have a serum sodium level below 130 mEq/L or a serum creatinine level above 1.6 mg/dl. Route Onset Peak Duration P.O. 1 hr 4–6 hr About 24 hr I.V. 15 min 1–4 hr About 6 hr

Mechanism of Action

May reduce blood pressure by affecting the renin-angiotensin-aldosterone system. By inhibiting angiotensin-convering enzyme (ACE), enalapril:

prevents conversion of angiotensin I to angiotensin II, a potent vasoconstrictor that also stimulates the adrenal cortex to enalapril maleate 367 E F secrete aldosterone

may inhibit renal and vascular production of angiotensin II

decreases the serum angiotensin II level and increases serum renin activity, which decreases aldosterone secretion and slightly increases serum potassium level and fluid loss

decreases vascular tone and blood pressure

inhibits aldosterone release, which reduces sodium and water reabsorption and increases their excretion, further reducing blood pressure.

Contraindications

History of angioedema from previous ACE inhibitor; hypersensitivity to enalapril, enalaprilat, or their components

Interactions

allopurinol, bone marrow depressants (such as amphotericin B and methotrexate), procainamide, systemic corticosteroids: Possibly increased risk of fatal neutropenia or agranulocytosis cyclosporine, potassium-sparing diuretics, potassium supplements: Increased risk of hyperkalemia diuretics, other antihypertensives: Additive hypotensive effects lithium: Increased blood lithium level and lithium toxicity
NSAIDs: Possibly reduced antihypertensive effects of enalapril and enalaprilat sodium aurothiomalate: Increased risk of nitritoid reactions, such as facial flushing, nausea, vomiting, and hypotension sympathomimetics: Possibly reduced therapeutic effects of enalapril and enalaprilat potassium-containing salt substitutes: Increased risk of hyperkalemia
alcohol use: Possibly additive hypotensive effect

Side Efect

CNS: Ataxia, confusion, depression, dizziness, dream disturbances, fatigue, headache, insomnia, nervousness, peripheral neuropathy, somnolence, stroke, syncope, vertigo, weakness
CV: Angina, arrhythmias, cardiac arrest, hypotension, MI, orthostatic hypotension, palpitations, pulmonary embolism and infarction, Raynaud’s phenomenon
EENT: Blurred vision, conjunctivitis, dry eyes and mouth, glossitis, hoarseness, lacrimation, loss of smell, pharyngitis, rhinorrhea, stomatitis, taste perversion, tinnitus
ENDO: Gynecomastia
GI: Abdominal pain, anorexia, constipation, diarrhea, hepatic failure, hepatitis, ileus, indigestion, melena, nausea, pancreatitis, vomiting
GU: Flank pain, impotence, oliguria, renal failure, UTI
MS: Muscle spasms
RESP: Asthma, bronchitis, bronchospasm, cough, dyspnea, pneumonia, pulmonary edema, pulmonary infiltrates, upper respiratory tract infection
SKIN: Alopecia, diaphoresis, erythema multiforme, exfoliative dermatitis, flushing, pemphigus, photosensitivity, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, herpes zoster, hyperkalemia

Cautions

Use enalapril and enalaprilat cautiously in patients with impaired renal function. Avoid giving drug to children with a GFR less than 30 ml/min/1.73 m2.

For children who can’t swallow tablets, consult with prescriber and pharmacist about preparing an oral suspension from tablets as directed by manufacturer.

Administer each I.V. dose over at least 5 minutes.

Measure patient’s blood pressure immediately after first dose and frequently for at least 2 hours thereafter. If hypotension requires a dosage reduction, monitor blood pressure frequently for 2 hours after reduced dosage is administered and for another hour after blood pressure has stabilized.

Monitor blood pressure regularly during therapy. If hypotension develops, place patient in a supine position and expect to give I.V. normal saline solution or other volume expander as prescribed.

Monitor patient’s heart rate and rhythm. Expect to obtain repeated 12-lead ECG tracings.

Monitor laboratory test results to check hepatic and renal function, leukocyte count, and serum potassium level. enalapril maleate 368

Monitor patient closely for angioedema of the face, lips, tongue, glottis, larynx, and limbs. For angioedema of the face and lips, stop drug and give an antihistamine, as prescribed. If tongue, glottis, or larynx is involved, assess patient for airway obstruction and prepare to give epinephrine 1:1,000 (0.3 to 0.5 ml) subcutaneously and maintain a patent airway.

PATIENT SAFTY

Advise patient to take enalapril or enalaprilat at the same time each day.

Instruct patient not to split, crush, or chew tablets.

Inform patient that light-headedness and fainting may occur, especially during first few days of therapy. Advise him to change position slowly and avoid hazardous activities until drug’s CNS effects are known.

Inform patient that diarrhea, excessive sweating, vomiting, and other conditions may cause dehydration, which can lead to dizziness, fainting, and very low blood pressure during therapy. Urge sufficient fluid intake to prevent dehydration and related

Side Efect

. If diarrhea or vomiting is severe or prolonged, instruct patient to notify prescriber.

Urge patient to immediately notify prescriber if angioedema and other adverse reactions, including persistent dry cough, occur.

Advise patient to consult prescriber before using salt substitutes, potassium supplements, or other (including OTC ) while taking drug.
WARNING Caution women of childbearing age that they should use a reliable form of contraception and should notify prescriber immediately if pregnancy is suspected because enalapril may cause fetal harm and should be discontinued.

Category

Chemical class: Fluoroquinolone
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To treat gonorrhea
Adults.400 mg as a single dose. To treat uncomplicated UTI
Adults.200 mg every 12 hr for 7 days. To treat complicated UTI
Adults.400 mg every 12 hr for 14 days.
DOSAGE ADJUSTMENT Dosage reduced by half in patients with creatinine clearance of 30 ml/min/1.73 m2or less.

Contraindications

History of tendinitis or tendon rupture, hypersensitivity to enoxacin or any quinolone antibiotic

Interactions

aluminum-, calcium-, or magnesiumcontaining antacids; didanosine (chewable or buffered tablets); ferrous sulfate; magnesiumcontaining laxatives; sucralfate; zinc: Interference with enoxacin absorption, decreased blood enoxacin level bismuth: Decreased enoxacin bioavailability (by about 25% if given with or up to 60 minutes after enoxacin) cyclosporine: Possibly increased blood cyclosporine level digoxin: Increased serum digoxin level and risk of digitalis toxicity
NSAIDs: Possibly increased risk of CNS stimulation and seizures
theophylline: Interference with theophylline metabolism, increased risk of theophylline toxicity
warfarin: Possibly increased anticoagulant effect and increased risk of bleeding caffeine: Decreased caffeine clearance, increased adverse effects of caffeine, increased blood enoxacin level

Side Efect

CNS: Dizziness, drowsiness, hallucinations, headache, insomnia, nervousness, seizures, vertigo
EENT: Taste perversion
GI: Abdominal pain, diarrhea, indigestion, nausea, pseudomembranous colitis, vomiting
GU: Vaginitis
MS: Tendinitis, tendon rupture
SKIN: Photosensitivity, pruritus, rash
Other: Anaphylaxis enoxacin 369 E F

Cautions

Be aware that enoxacin shouldn’t be given to a patient under age 18 because it may cause arthropathy.

Use drug cautiously in patients with a history of or susceptibility to seizures.

Obtain a specimen for culture and sensitivity tests, as ordered, but expect to begin therapy before results are available.

Monitor patient closely for signs and symptoms of anaphylaxis after first dose: shock, dyspnea, facial or laryngeal edema, loss of consciousness, paresthesia, pruritus, and urticaria. If they occur, stop enoxacin immediately, notify prescriber, and prepare to treat symptoms.

Ask if patient has a history of seizures. Take seizure and safety precautions because drug may induce seizures and other adverse CNS reactions after a single dose.

Report severe or prolonged diarrhea, which may indicate pseudomembranous colitis.

Watch for pain, inflammation, and tendon rupture, especially in shoulders, hands, and ankles.

If patient has gonorrhea, expect to obtain a serologic test for syphilis at diagnosis and 3 months after enoxacin therapy ends.

PATIENT SAFTY

Stress the importance of taking the full course of enoxacin exactly as prescribed, even if patient feels better before it’s finished.

Instruct patient to take drug at the same times each day—1 hour before or 2 hours after meals—with 8 oz of water.

Urge patient to avoid potentially hazardous activities until CNS effects of enoxacin are known.

Advise patient to notify prescriber if symptoms don’t improve within a few days.

Urge patient to drink plenty of fluids but to avoid caffeine during therapy.

Caution patient not to take aluminum-, calcium-, or magnesium-containing antacids; bismuth; didanosine (chewable or buffered tablets), if prescribed; or products that contain iron or zinc for 8 hours before or 2 hours after taking enoxacin.

Tell patient to avoid direct sunlight, to use sunscreen and wear protective clothing outdoors, and to report photosensitivity.

Instruct patient to stop taking enoxacin and notify prescriber immediately if a rash or other allergic reaction develops.

Instruct patient to take a missed dose as soon as he remembers, unless it’s nearly time for the next. Warn against doubling the dose.

Tell patient to report tendon pain or inflammation, to stop enoxacin, and to rest until tendinitis or tendon rupture is ruled out. enoxacin 370 Normal DNA replication Inhibited DNA replication Enoxacin inhibiting DNA gyrase Original DNA molecule DNA gyrase DNA gyrase New DNA blocked New DNA molecule New DNA molecule Normal DNA replication Inhibited DNA replication Enoxacin inhibiting DNA gyrase Original DNA molecule DNA gyrase DNA gyrase New DNA blocked New DNA molecule New DNA molecule

Mechanism of Action

Normally, the enzyme DNA gyrase is responsible for unwinding and supercoiling bacterial DNA before replication, as shown at left. Enoxacin inhibits DNA gyrase, as shown at right, disrupting bacterial replication and causing cell death.

Category

Chemical class: Low-molecular-weight heparin
Therapeutic class: Antithrombotic

Pregnancy category: B

Indications

To prevent deep vein thrombosis (DVT) after hip or knee replacement and for continued prophylaxis after hospitalization for hip replacement SUBCUTANEOUS INJECTION
Adults.30 mg every 12 hr, starting 12 to 24 hr after surgery for up to 14 days. Or, 40 mg daily, starting 9 to 15 hr after hip replacement surgery. Prophylaxis: 40 mg daily for 3 wk. To prevent DVT after abdominal surgery for patients with thromboembolic risk factors (over age 40, obesity, general anesthesia lasting longer than 30 minutes, cancer, or a history of DVT or pulmonary embolism) SUBCUTANEOUS INJECTION
Adults.40 mg daily, starting 2 hr before surgery and lasting 7 to 10 days. To prevent ischemic complications of unstable angina and non–Q-wave MI SUBCUTANEOUS INJECTION
Adults.1 mg/kg every 12 hr with 100 to 325 mg of aspirin daily for 2 to 8 days or until condition is stable.
DOSAGE ADJUSTMENT Dosage reduced to 30 mg daily if creatinine clearance is less than 30 ml/min/1.73 m2and patient is receiving drug as prophylaxis in abdominal, hip, or knee replacement surgery or is acutely ill. Reduced to 1 mg/kg daily if creatinine clearance is less than 30 ml/min/ 1.73 m2and drug is given with aspirin to prevent ischemic complications of unstable angina and non–Q-wave MI, with warfarin as inpatient treatment for acute DVT with or without pulmonary embolism, or with warfarin as outpatient treatment of acute DVT without pulmonary embolism. To treat acute ST-segment–elevation MI (STEMI) I.V. INJECTION, THEN SUBCUTANEOUS INJECTION
Adults. 30 mg I.V. as a single dose, followed by 1 mg/kg subcutaneously (maximum, 100 mg for first two doses). Then, 1 mg/kg subcutaneously every 12 hr.
DOSAGE ADJUSTMENT If patient also receives a thrombolytic, enoxaparin should be given 15 to 30 min before and 30 min after fibrinolytic therapy starts. If patient has percutaneous coronary intervention, give 0.3-mg/ kg I.V. bolus if last enoxaparin dose was given more than 8 hr before balloon inflation. Route Onset Peak Duration SubQ Unknown 3–5 hr Up to 24 hr

Mechanism of Action

Potentiates the action of antithrombin III, a coagulation inhibitor. By binding with antithrombin III, enoxaparin rapidly binds with and inactivates clotting factors (primarily thrombin and factor Xa). Without thrombin, fibrinogen can’t convert to fibrin and clots can’t form.

Incompatibilities

Don’t mix enoxaparin with other I.V. fluids or .

Contraindications

Active major bleeding; hypersensitivity to benzyl alcohol (if only the multidose vial is available), enoxaparin, heparin (including low-molecular-weight heparins), or pork products; thrombocytopenia and positive antiplatelet antibody test while taking lowmolecular-weight heparins

Interactions

cefamandole, cefoperazone, cefotetan, plicamycin,
valproic acid: Possibly increased risk of hemorrhage NSAIDs; oral anticoagulants; platelet aggregation inhibitors, such as aspirin, dipyridamole, sulfinpyrazone, and ticlopidine; thrombolytics, such as alteplase, anistreplase, streptokinase, and urokinase: Possibly increased risk of bleeding and of spinal or epidural hematoma

Side Efect

CNS: Confusion, epidural or spinal hematoma, fever, paralysis, stroke
CV: Atrial fibrillation, congestive heart failure, hyperlipidemia, peripheral edema
EENT: Epistaxis enoxaparin sodium 371 E F
GI: Bloody stools, diarrhea, elevated liver function test results, hematemesis, melena, nausea, vomiting
GU: Hematuria, menstrual irregularities
HEME: Anemia, hemorrhage, thrombocytopenia
RESP: Dyspnea, pneumonia, pulmonary edema or embolism
SKIN: Cutaneous vasculitis, ecchymosis, persistent bleeding or oozing from mucous membranes or surgical wounds, pruritus, skin necrosis at injection site or distant from injection site, urticaria, vesiculobullous rash
Other: Anaphylaxis; hyperkalemia; injection site erythema, hematoma, irritation, and pain

Cautions

Use enoxaparin with extreme caution in patients with a history of heparin-induced thrombocytopenia or an increased risk of hemorrhage, as from bacterial endocarditis; congenital or acquired bleeding disorder; active ulcerative or angiodysplastic GI disease; hemorrhagic stroke; recent brain, spinal, or ophthalmologic surgery; or concurrent treatment with a platelet inhibitor.

Use cautiously in those with bleeding diathesis, diabetic retinopathy, hepatic or renal impairment, recent GI ulceration or hemorrhage, or uncontrolled hypertension. Expect delayed elimination in elderly patients and those with renal insufficiency.

Drug isn’t recommended for patients with prosthetic heart valves, especially pregnant women, because of risk of prosthetic valve thrombosis. If enoxaparin is needed, monitor peak and trough anti-factor Xa levels often and adjust dosage as needed.

Use multidose vials cautiously in pregnant women because benzyl alcohol may cross the placenta and cause fetal harm.

Don’t give drug by I.M. injection.
WARNING If patient is receiving enoxaparin with epidural or spinal anesthesia or spinal puncture, watch closely for development of spinal hematoma, which may cause long-term or permanent paralysis. If you see evidence of neurologic impairment, such as changes in sensory or motor function, notify prescriber immediately because urgent care is needed to minimize hematoma’s effect. Risk of spinal or epidural hematoma during enoxaparin therapy is increased by indwelling epidural catheters, concurrent use of other that affect hemostatis, a history of traumatic or repeated epidural or spinal punctures, or a history of spinal deformity or spinal surgery.

Expect to give drug with aspirin to patient with unstable angina, STEMI, and non–Qwave MI. To minimize risk of bleeding after vascular procedures, give enoxaparin at recommended intervals.

After percutaneous revascularization procedure, it is important to achieve hemostasis at the puncture site. A closure device may be removed right away; however, if a manual compression method is used, the sheath should be removed 6 hours after last enoxaparin dose. If enoxaparin therapy will continue, give next scheduled dose no sooner than 6 to 8 hours after sheath removal.

Watch closely for bleeding. Notify prescriber immediately if platelet count falls below 100,000/mm3. Expect to stop drug and start treatment if patient has a thromboembolic event, such as a stroke.

Test stool for occult blood, as ordered.

Keep protamine sulfate nearby in case of accidental overdose.

Check serum potassium level for elevation, especially in patients with renal impairment or concurrent use of potassium-sparing diuretics.

PATIENT SAFTY

Advise patient to notify prescriber about

Side Efect

, especially bleeding.

Instruct patient to seek immediate help for evidence of thromboembolism, such as neurologic changes and severe shortness of breath.

Stress the importance of complying with follow-up visits with prescriber.

Teach patient or family member how to give enoxaparin at home, if needed. Show patient how to give by deep subcutaneous injection while lying down. Instruct him not to expel air bubble from a prefilled syringe to avoid losing some of the drug. Tell him to insert the entire needle into a skin fold held between the thumb and forefinger. Remind him to alternate injection sites between the left and right anterolateral abdominal wall.

To minimize bruising, caution patient not enoxaparin sodium 372 to rub the site after giving the injection.

Review safe handling and disposal of syringes and needles.

Category

Chemical class: COMT inhibitor
Therapeutic class: Antidyskinetic

Pregnancy category: C

Indications

As adjunct to manage symptoms of Parkinson’s disease
Adults. 200 mg with each dose of carbidopa and levodopa. Maximum: 1,600 mg daily.

Mechanism of Action

Inhibits peripheral catechol-O-methyltransferase (COMT), the major metabolizing enzyme for levodopa. During levodopa metabolism, COMT causes the formation of a levodopa metabolite that reduces the effectiveness of levodopa. By inhibiting COMT, entacapone leads to higher sustained blood levels of levodopa and its increased availability for diffusion into the CNS, where it is converted to dopamine. By replenishing dopamine stores, entacapone increases dopaminergic stimulation in the brain and reduces the symptoms of Parkinson’s disease. Carbidopa is given with levodopa because it inhibits the peripheral distribution of levodopa, making more levodopa available for transport to the brain.

Contraindications

Hypersensitivity to entacapone or its components, use within 14 days of nonselective MAO inhibitor therapy

Interactions

ampicillin, chloramphenicol, cholestyramine, erythromycin, probenecid,
rifampin: Decreased biliary excretion of entacapone apomorphine, bitolterol, dobutamine, dopamine, epinephrine, isoetharine, isoproterenol, methyldopa, norepinephrine: Possibly increased heart rate, arrhythmias, and excessive changes in blood pressure MAO inhibitors (nonselective): Possibly inhibited entacapone metabolism

Side Efect

CNS: Agitation, anxiety, asthenia, dizziness, dyskinesia, fatigue, hallucinations, hyperkinesia, hypokinesia, somnolence
EENT: Dry mouth
GI: Abdominal pain, constipation, diarrhea, indigestion, gastritis, nausea
GU: Brown-orange urine
MS: Back pain
RESP: Dyspnea
SKIN: Diaphoresis, purpura
Other: Intense urges to perform certain acts, such as gambling or sex

Cautions

WARNING Be aware that entacapone should not be discontinued abruptly because doing so may precipitate signs and symptoms resembling those of neuroleptic malignant syndrome, such as fever, muscle rigidity, altered level of consciousness, confusion, and elevated creatine kinase level. Patients may also experience a rapid reemergence of parkinsonian symptoms.

Monitor patient for drug-induced diarrhea during first 4 to 12 weeks of therapy.

Help patient with activities as needed because drug may increase risk of orthostatic hypotension or syncope.

Watch for worsening dyskinesia because entacapone potentiates dopaminergic adverse effects of levodopa.

Drug may be taken with selective MAO inhibitors, such as selegiline.

Assess patient for skin changes regularly because risk of melanoma is increased in those with Parkinson’s disease. It isn’t clear whether increased risk results from the disease or used to treat it.

PATIENT SAFTY

Instruct patient to always take entacapone with carbidopa and levodopa because it has no antidyskinetic effect of its own.

Inform patient that dizziness and sleepiness are more common at beginning of treatment, especially in those with hypotension.

Advise patient not to participate in potentially hazardous activities until drug’s CNS effects are known, especially if he’s also taking CNS depressants.

If patient is scheduled for surgery, instruct him to inform surgeon and anesthesioloentacapone 373 E F gist about entacapone use before the prcedure because COMT inhibitors such as entacapone may interact with some used in surgical procedures.

Caution patient that entacapone may increase adverse effects of carbidopa and levodopa, such as nausea and uncontrolled movements. If these adverse effects do increase, advise him to contact prescriber immediately because carbidopa and levodopa dosage may need to be lowered.

Inform patient that urine may turn brown-orange while he’s taking entacapone but that this is a harmless effect.

Urge patient to have regular skin examinations by a dermatologist or other qualified health professional.

Advise patient to notify prescriber about intense urges, including those for gambling or sex. Dosage may need to be reduced or drug discontinued.

Category

Chemical class: Catecholamine
Therapeutic class: Antianaphylactic, bronchodilator, cardiac stimulant, vasopressor

Pregnancy category: C

Indications

To treat bronchospasm INHALED SOLUTION(EPINEPRHINE) Adults and children age 4 and over. 1 to 3 inhalations (10 drops) by hand-bulb nebulizer no more than every 3 hr. INHALED SOLUTION(RACEPINEPHRINE) Adults and children age 4 and over. 3 inhalations of 0.5 ml (10 drops) by handbulb nebulizer, or 0.2 to 0.5 ml (4 to 10 drops) of diluted solution given over 15 min by jet nebulizer; repeated after 3 to 4 hr, if needed. ORAL INHALED AEROSOL(EPINEPHRINE BITARTRATE) Adults and children age 4 and over. 1 inhalation (160 mcg) repeated after 1 min, if needed; then repeated after at least 3 hr. ORAL INHALER(EPINEPHRINE) Adults and children age 4 and over. 1 inhalation (200 to 275 mcg) repeated after at least 1 min, if needed; then repeated after at least 3 hr. To treat croup INHALED SOLUTION(RACEPINEPHRINE) Children. 0.05 ml/kg diluted to 3 ml in normal saline solution and given over 15 min every 2 hr, as needed. Maximum: 0.5 ml/dose. To treat anaphylaxis
IV: Adults and adolescents.100 to 250 mcg given slowly. I.M.OR SUBCUTANEOUS INJECTION Adults and adolescents. 100 to 500 mcg repeated every 10 to 15 min, as needed. Maximum: 1 mg/dose; three doses. Children.10 mcg/kg repeated every 15 min for three doses. Maximum: 300 mcg/dose. To treat severe anaphylactic shock
IV:
Adults.1 mcg/min titrated to 2 to 10 mcg/ min for desired hemodynamic response. To treat cardiac arrest
I.V.INJECTION
Adults. 0.5 to 1 mg every 3 to 5 min during resuscitation. Children.10 mcg/kg followed by 100 mcg/ kg every 3 to 5 min, if needed. If two doses produce no response, subsequent doses are increased to 200 mcg/kg every 5 min. Neonates. 10 to 30 mcg/kg every 3 to 5 min.

Mechanism of Action

Acts on alpha and beta receptors. This nonselective adrenergic agonist stimulates:

alpha1receptors, which constricts arteries and may decrease bronchial secretions

presynaptic alpha2receptors, which inhibits norepinephrine release by way of epinephrine 374 negative feedback

postsynaptic alpha2receptors, which constricts arteries

beta1receptors, which induces positive chronotropic and inotropic responses

beta2receptors, which dilates arteries, relaxes bronchial smooth muscles, increases glycogenolysis, and prevents mast cells from secreting histamine and other substances, thus reversing bronchoconstriction and edema. Route Onset Peak Duration I.V., I.M. Rapid Unknown 1–2 min SubQ 5–10 min In 20 min Short Oral 1–5 min In 5–15 Up to inhalation min 3 hr

Incompatibilities

Don’t mix epinephrine with alkalies or oxidizing agents, including bromine, chlorine, chromates, iodine, metal salts (as from iron), nitrites, oxygen, and permanganates, because these substances can destroy epinephrine.

Contraindications

Cerebral arteriosclerosis, coronary insufficiency, counteraction of phenothiazineinduced hypotension, dilated cardiomyopathy, general anesthesia with halogenated hydrocarbons or cyclopropane, hypersensitivity to epinephrine or its components, labor, angle-closure glaucoma, organic brain damage, shock (nonanaphylactic)

Interactions

alpha-adrenergic blockers, with alphaadrenergic action, rapid-acting vasodilators: Blockage of epinephrine’s alpha-adrenergic effect, possibly causing severe hypotension and tachycardia amyl nitrite, nitrates: Decreased antianginal effects antihypertensives, diuretics used to treat hypertension: Decreased antihypertensive effects
beta blockers: Mutual inhibition of therapeutic effects, possibly severe hypertension and cerebral hemorrhage chlorpheniramine, diphenhydramine, levothyroxine, MAO inhibitors, tricyclic antidepressants, tripelennamine: Possibly increased effects of epinepherine digoxin, diuretics,
quinidine: Increased risk of arrhythmias dihydroergotamine, ergoloid mesylates, ergonovine, ergotamine, methylergonovine, methysergide, oxytocin: Increased risk of vasoconstriction, causing gangrene, peripheral vascular ischemia, or severe hypertension ergot alkaloids: Possibly reversed pressor effects of epinephrine hydrocarbon inhalation anesthetics: Increased risk of severe atrial and ventricular arrhythmias insulin, oral antidiabetic : Decreased effects of these
MAO inhibitors: Possibly increased vasopressor effect of epinephrine and hypertensive crisis maprotiline, tricyclic antidepressants: Potentiated cardiovascular effects of epinephrine, possibly causing arrhythmias, hyperpyrexia, severe hypertension, or tachycardia sympathomimetics: Additive CNS stimulation, increased cardiovascular effects of either drug thyroid hormones: Increased effects of either drug xanthines: CNS stimulation and toxic effects

Side Efect

CNS: Anxiety, apprehensiveness, chills, fever, dizziness, drowsiness, hallucinations, headache, insomnia, light-headedness, nervousness, restlessness, seizures, stroke, temporary worsening of Parkinson’s disease, tremor, weakness
CV: Arrhythmias, including ventricular fibrillation; chest discomfort or pain; fast, irregular, or slow heartbeat; palpitations; severe hypertension; tachycardia
EENT: Blurred vision, dry mouth or throat, miosis
ENDO: Hyperglycemia in diabetics
GI: Anorexia, heartburn, nausea, vomiting
GU: Dysuria
MS: Muscle twitching, severe muscle spasms
RESP: Dyspnea
SKIN: Cold skin, diaphoresis, ecchymosis, flushed or red face or skin, pallor, tissue necrosis
Other: Hyperkalemia; hypokalemia; injecepinephrine 375 E F tion site coldness, hypoaesthesia, pain, pallor, and stinging

Cautions

Use epinephrine with extreme caution in patients with angina, arrhythmias, asthma, degenerative heart disease, or emphysema. Epinephrine’s inotropic effect equals that of dopamine and dobutamine; its chronotropic effect exceeds that of both.

Use drug cautiously in elderly patients and those with cardiovascular disease (other than listed above), diabetes mellitus, hypertension, hyperthyroidism, prostatic hypertrophy, and psychoneurologic disorders.

Be aware that some preparations contain sulfites, which may cause allergic-type reactions. However, the presence of sulfites in epinephrine should not deter its use in a patient with anaphylaxis, even if patient is sensitive to sulfites. Monitor patient closely for adverse effects.

Dilute the 1:1,000 (1-mg/ml) solution of parenteral epinephrine before I.V. use.

Shake suspension thoroughly before withdrawing dose; refrigerate it between uses.

Inspect epinephrine solution or suspension before use. If it’s pink or brown, air has entered a multidose vial. If it’s discolored or contains particles, discard it. Also discard unused portions of parenteral epinephrine.

For injection, rotate sites because repeated injections in the same site may cause vasoconstriction and localized necrosis.

Be aware that drug shouldn’t be given by intra-arterial injection because marked vasoconstriction may cause gangrene.

Avoid giving injection into buttocks bec ause drug may be less effective when given there, especially for treating anaphylaxis.

Monitor patient for potassium imbalances. Initially, hyperkalemia occurs when hepatocytes release potassium. Hypokalemia may quickly follow as skeletal muscles take up potassium.

To minimize insomnia, give last dose a few hours before bedtime.
WARNING To treat cardiac arrest, at least twice the peripheral I.V. dose of epinephrine may be given by endotracheal instillation. Two dilutions are needed for this regimen; use great caution to avoid making medication errors.

PATIENT SAFTY

Warn patient not to exceed recommended dosage or to shorten interval because of the risk of

Side Efect

and tolerance.

Advise patient to notify prescriber if symptoms don’t improve or if they improve but then worsen.

Instruct patient to take the day’s last dose a few hours before bedtime to avoid insomnia.

Caution patient not to use inhalation solution that is pink or brown or that contains particles.

Teach patient how to use oral inhaler or inhalation solution, as needed.

If patient also uses an oral corticosteroid inhaler, instruct him to use epinephrine inhaler first, wait 5 minutes, and then use corticosteroid inhaler to increase effectiveness.

Teach patient and family how to administer epinephrine subcutaneously in an emergency. Tell them to inject drug into anterolateral aspect of the thigh, through the clothing if necessary. Explain that solution is light sensitive and should be stored in the carrying case and at room temperature. Tell them not to refrigerate drug and to replace solution if it discolors.

Caution patient to avoid accidental injecting drug into his fingers, hands, toes, or feet because epinephrine is a strong vasoconstrictor and could cause loss of blood flow to the area, resulting in gangrene. If accidental injection occurs in any of these areas, instruct patient to go immediately to nearest emergency room.

Advise patient to notify prescriber immediately if he has blurred vision, chest pain, trouble breathing, a fast or irregular heartbeat, or increased sweating.

Inform patient with diabetes that epinephrine may cause hyperglycemia. Inform patient with Parkinson’s disease that symptoms my temporarily worsen but this should not deter use of drug.

Category

Chemical class: Methyl ester eplerenone 376
Therapeutic class: Antihypertensive

Pregnancy category: B

Indications

To improve survival of stable patients with left ventricular systolic dysfunction and congestive heart failure after an acute MI
Adults. Initial: 25 mg daily, increased to 50 mg daily within 4 wk, if needed. To treat hypertension alone or with other antihypertensive
Adults. Initial: 50 mg daily, increased to 50 mg b.i.d. after 4 wk, if needed.
DOSAGE ADJUSTMENT For patients taking weak CYP450 3A4 inhibitors, such as erythromycin, saquinavir, verapamil, and fluconazole, initial dosage reduced to 25 mg daily.

Mechanism of Action

Blocks the binding of aldosterone at its mineralocorticoid receptor sites located in the kidneys, heart, blood vessels, and brain. This action decreases blood pressure by preventing aldosterone from inducing sodium reabsorption and possibly other mechanisms that contribute to raising blood pressure.

Contraindications

Hyperkalemia (serum potassium level greater than 5.5. mEq/L); hypersensitivity to eplerenone or its components; renal insufficiency (serum creatinine level greater than 2.0 mg/dl in men or 1.8 mg/dl in women or creatinine clearance less than 50 ml/min/1.73 m2); type 2 diabetes mellitus complicated by microalbuminuria; use of potassium supplements, potassium-sparing diuretics, or strong CYP3A4 inhibitors, such as ketoconazole or itraconazole

Interactions

ACE inhibitors, angiotensin II receptor antagonists: Increased risk of hyperkalemia CYP450 3A4 inhibitors: Increased blood level and effect of eplerenone lithium: Possibly lithium toxicity
NSAIDs: Possibly reduced antihypertensive effect of eplerenone grapefruit: Possibly increased blood level and effect of eplerenone

Side Efect

CNS: Dizziness, fatigue, headache
CV: Angina pectoris, hypercholesterolemia, hypertriglyceridemia, MI
ENDO: Gynecomastia, mastodynia
GI: Abdominal pain, diarrhea, increased liver enzyme levels
GU: Albuminuria, elevated BUN and serum creatinine levels, vaginal bleeding
RESP: Cough
Other: Flulike symptoms, hyperkalemia, hyponatremia, increased uric acid level

Cautions

Monitor patient’s blood pressure regularly to evaluate eplerenone effectiveness.

Monitor patient’s serum potassium level every 2 weeks for the first month or two of therapy and monthly thereafter, as ordered.

Be aware that patients who take an ACE inhibitor or an angiotensin II receptor antagonist during eplerenone therapy have an increased risk of hyperkalemia.

PATIENT SAFTY

Caution patient not to use potassiumcontaining supplements or salt substitutes because increased potassium levels can lead to serious

Side Efect

to eplerenone.

Urge patient to tell all prescribers about eplerenone use because of possible interactions.

Category

Chemical class: 165–amino acid glycoprotein identical to human erythropoietin
Therapeutic class: Antianemic

Pregnancy category: C

Indications

To treat anemia from renal failure I.V.OR SUBCUTANEOUS INJECTION Adults and adolescents. Initial: 50 to 100 units/kg 3 times/wk, increased by epoetin alfa 377 E F 25 units/kg after 8 wk if hematocrit hasn’t risen by 5 or 6 points or is below desired range (30% to 36%). Maintenance: Dosage gradually decreased by 25 units/kg at 4-wk intervals or longer to lowest dose that keeps hematocrit at 30% to 36%. Maximum: 300 units/kg 3 times/wk. Children on dialysis. 50 units/kg 3 times/ wk; increased after 8 wk if hematocrit hasn’t risen by 5 or 6 points and is still below desired range of 30% to 36%. Maintenance: Dosage gradually decreased to lowest dose that keeps hematocrit at 30% to 36%. To treat anemia in HIV-infected patients who take zidovudine I.V.OR SUBCUTANEOUS INJECTION Adults with serum erythropoietin level of 500 mU/ml or less who receive 4,200 mg or less of zidovudine/wk. Initial: 100 units/ kg 3 times/wk, increased by 50 to 100 units/ kg every 4 to 8 wk after 8 wk of therapy. Maintenance: Dosage gradually titrated to maintain desired response, based on such factors as variations in zidovudine dosage and occurrence of infection or inflammation. Maximum: 300 units/kg 3 times/wk. To treat anemia from chemotherapy SUBCUTANEOUS INJECTION
Adults. Initial: 150 units/kg 3 times/wk. Dosage decreased by 25% if hemoglobin level approaches 12 g/dl or increases more than 1 g/dl in any 2-wk period. Dose withheld if hemoglobin exceeds 13 g/dl and resumed at 25% less than previous dose after hemoglobin has fallen to 12 g/dl. Dosage increased to 300 units/kg 3 times/ wk after 8 wk if response is inadequate. Maximum: 300 units/kg 3 times/wk. Or, 40,000 units weekly. Dosage decreased by 25% if hemoglobin level approaches 12 g/dl or increases more than 1 g/dl in any 2-wk period. Dose withheld if hemoglobin level exceeds 13 g/dl and resumed at 25% less than previous dose after hemoglobin has fallen to 12 g/dl. Dosage increased to 60,000 units weekly after 8 wk if hemoglobin level has not increased at least 1 g/dl without RBC transfusion. To reduce the need for blood transfusion in anemic patients having surgery SUBCUTANEOUS INJECTION
Adults.300 units/kg daily for 10 days before surgery, on day of surgery, and 4 days after surgery; or 600 units/kg/wk starting 3 wk before surgery for a total of 3 doses. Dose of 300 units/kg repeated on day of surgery.
DOSAGE ADJUSTMENT For patients with anemia from renal failure, dosage temporarily reduced or drug discontinued if hematocrit reaches or exceeds 36%; drug is resumed at a lower dose when hematocrit returns to desired range. For patients with anemia from zidovudine use, therapy temporarily stopped if hematocrit reaches or exceeds 40% and is resumed at a 25% lower dose when hematocrit returns to desired range. Route Onset Peak Duration I.V., In 2–6 wk In 2 mo About SubQ 2 wk

Mechanism of Action

Stimulates the release of reticulocytes from the bone marrow into the bloodstream, where they develop into mature RBCs.

Incompatibilities

Don’t mix epoetin alfa with any other drug.

Contraindications

Hypersensitivity to human albumin or products made from mammal cells, uncontrolled hypertension

Interactions

antihypertensives: Increased blood pressure (to hypertensive level), especially when hematocrit rises rapidly heparin: Increased heparin requirement in hemodialysis patients iron supplements: Increased iron requirement and need for increased dose

Side Efect

CNS: Anxiety, asthenia, dizziness, fatigue, fever, headache, insomnia, paresthesia, seizures, stroke
CV: Chest pain, deep vein thrombosis, edema, hypertension, MI, tachycardia
GI: Constipation, diarrhea, indigestion, nausea, vomiting
GU: UTI
HEME: Polycythemia
MS: Arthralgia, bone pain, muscle weakness
RESP: Cough, dyspnea, pulmonary congestion, upper respiratory tract infection
SKIN: Rash, pruritus, urticaria
Other: Flulike symptoms, hyperkalemia, injection site reaction, trunk pain epoetin alfa 378

Cautions

Use epoetin alfa cautiously in patients who have conditions that could decrease or delay response to drug, such as aluminum intoxication, folic acid deficiency, hemolysis, infection, inflammation, iron deficiency, malignant neoplasm, osteitis (fibrosa cystica), or vitamin B12deficiency.

Also use drug cautiously in patients with cardiovascular disorders caused by hypertension, a history of porphyria or seizures, vascular disease, or a hematologic disorder, such as hypercoagulation, myelodysplastic syndrome, or sickle cell disease.
WARNING Multidose vial of epoetin contains benzyl alcohol, which can cause a fatal toxic syndrome in neonates and immature infants characterized by CNS, respiratory, circulatory, and renal impairment and metabolic acidosis.

Use lowest possible dose in cancer patients because drug has shortened survival rate and increased tumor progression in patients with certain types of cancers, such as breast, non-small cell lung, head and neck, and lymphoid cancers. Drug should only be used to treat anemia caused by myelosuppressive chemotherapy in cancer patients.

Don’t shake vial while preparing to avoid denaturing glycoprotein, inactivating drug.

Discard unused portion of single-dose vial because it contains no preservatives. Discard unused portion of multidose vial after 21 days.

Baseline hemoglobin level should be above 10 but below 13 g/dl if drug is given to patient scheduled for surgery. Watch closely throughout surgical period for deep vein thrombosis, especially in patients not receiving prophylactic anticoagulation, because risk increases.
WARNING Target hemoglobin shouldn’t exceed 12 g/dl when treating anemia in patients with chronic renal failure. Exceeding 12 g/dl increases risk of lifethreatening adverse cardiovascular effects.

Expect to increase heparin dose if patient receives hemodialysis because epoetin alfa can increase the RBC volume, which could cause clots to form in the dialyzer, hemodialysis vascular access, or both.

Expect to give an iron supplement (I.V. iron dextran, if needed) because iron requirements rise when erythropoiesis consumes existing iron stores.

Monitor drug effectiveness by checking hematocrit, typically twice weekly until it stabilizes at 30% to 36%. After that, monitoring can be less frequent.

Take seizure precautions.

Check hemoglobin and hematocrit levels, as ordered, with twice-weekly measurements recommended for chronic renal failure patients and weekly measurements recommended for zidovudine-treated HIV-infected and cancer patients.

Risk of hypertensive or thrombotic complications increases if hematocrit rises more than 4 points in 2 weeks.

PATIENT SAFTY

Before epoetin alfa therapy starts, explain its serious adverse effects.

Teach patient how to administer drug and how to dispose of needles properly. Caution him against reusing needles.

Advise patient that the risk of seizures is highest during the first 90 days of epoetin alfa therapy. Urge him not to engage in hazardous activities during this time.

Stress the importance of complying with the dosage regimen and keeping follow-up medical appointments and appointments for laboratory tests.

Encourage patient to eat iron-rich

Review possible

Side Efect

, and urge patient to notify prescriber if he experiences chest pain, headache, hives, rapid heartbeat, rash, seizures, shortness of breath, or swelling.

Advise women of childbearing age to use effective contraception during therapy if pregnancy isn’t desired because menses may resume after epoetin alfa therapy.

Category

Chemical class: Natural prostaglandin
Therapeutic class: Antihypertensive, vasodilator

Pregnancy category: B

epoprostenol sodium 379 E F

Indications

To provide long-term treatment of primary pulmonary hypertension
IV:
Adults. Initial: 2 nanograms/kg/min, increased by 2 nanograms/kg/min every 15 min or longer until dose-limiting effects occur (abdominal, chest, or musculoskeletal pain; anxiety; bradycardia; dizziness; dyspnea; flushing; headache; hypotension; nausea; tachycardia; vomiting; or other adverse reactions). Maintenance: Dosage reduced by at least 4 nanograms/kg/min by continuous infusion.
DOSAGE ADJUSTMENT Infusion rate adjusted based on persistence, recurrence, or worsening of primary pulmonary hypertension and dose-related

Side Efect

.

Mechanism of Action

Directly relaxes vascular smooth muscles through its action as a natural prostaglandin. This results in arterial dilation and inhibition of platelet aggregation. These actions decrease pulmonary vascular resistance, increase cardiac index and oxygen delivery, and limit thrombus formation.

Incompatibilities

Don’t mix epoprostenol with other parenteral solutions or .

Contraindications

Hypersensitivity to epoprostenol or its components; long-term use in patients with heart failure caused by severe left ventricular systolic dysfunction; pulmonary edema that developed while establishing epoprostenol dosage

Interactions

anticoagulants, antiplatelet ,
NSAIDs: Increased risk of bleeding antihypertensives, diuretics, vasodilators: Decreased blood pressure

Side Efect

CNS: Anxiety, chills, confusion, dizziness, fever, headache, nervousness, paresthesia, syncope, weakness
CV: Bradycardia, chest pain, hypotension, tachycardia
GI: Abdominal pain, diarrhea, nausea, vomiting
HEME: Bleeding events, thrombocytopenia
MS: Arthralgia, jaw pain, myalgia
RESP: Dyspnea, hypoxia
SKIN: Flushing
Other: Flulike symptoms, injection site infection and pain, sepsis, weight loss or gain

Cautions

Use epoprostenol cautiously in elderly patients because they may have decreased hepatic, renal, or cardiac function, or other diseases or may receive other that can interact with epoprostenol.

Reconstitute drug only with sterile diluent that comes with package. Don’t dilute reconstituted epoprostenol.

To make 100 ml of reconstituted solution at 3,000 nanograms/ml, dissolve contents of 0.5-mg vial with 5 ml of diluent; withdraw 3 ml and add diluent to make 100 ml. To make 100 ml of solution at 5,000 nanograms/ml, dissolve contents of 0.5-mg vial with 5 ml of diluent; withdraw contents and add diluent to make 100 ml. To make 100 ml of solution at 10,000 nanograms/ml, dissolve contents of two 0.5-mg vials each with 5 ml of diluent; withdraw contents and add diluent to make 100 ml. To make 100 ml of solution at 15,000 nanograms/ml, dissolve contents of 1.5-mg vial with 5 ml of diluent; withdraw contents and add diluent to make 100 ml.

Give continuous infusion through central venous catheter. Use peripheral I.V. infusion only until central access established.

Use a small, lightweight, ambulatory infusion pump able to deliver 2 nanograms/ kg/min. It should have alarms for occlusion, end of infusion, and low battery. Use a polyvinyl chloride, polypropylene, or glass reservoir. Keep a backup pump and infusion set nearby to minimize disruptions in delivery.

At room temperature, administer a single container of reconstituted solution over 8 hours. For extended use at temperatures above 77° F (25° C), use a cold pouch with frozen gel packs to keep drug at 36° to 46° F (2° to 8° C) for 12 hours.

After a new infusion rate has been established, monitor patient closely for adverse reactions. Measure each blood pressure with patient standing and supine. Also, monitor heart rate for several hours after
DOSAGE ADJUSTMENT. epoprostenol sodium 380

During prolonged infusion, watch for dose-related

Side Efect

. If they develop, expect to decrease infusion by 2 nanograms/kg/min every 15 minutes, as prescribed, until reactions resolve.

Avoid abrupt withdrawal or a sudden large reduction in infusion rate, which could cause rebound pulmonary hypertension (asthenia, dizziness, dyspnea) or death.

Protect reconstituted drug from light, and refrigerate for no more than 48 hours. Discard solution that has been frozen or been refrigerated for more than 48 hours.

Watch for evidence of bleeding, especially if patient has other risk factors for bleeding, because epoprostenol is a potent inhibitor of platelet aggregation.

PATIENT SAFTY

Explain that epoprostenol is infused continuously through permanent indwelling central venous catheter by infusion pump.

Stress that patient must commit to longterm therapy, possibly for years.

Teach patient or caregiver how to reconstitute drug, administer it, and care for the permanent central venous catheter.

Urge patient to maintain prescribed infusion rate and to consult prescriber before altering it.

Caution patient that even brief interruptions in drug delivery may cause rapid worsening of symptoms.

Instruct patient to notify prescriber if

Side Efect

occur.

Make sure patient or caregiver has ready access to emergency phone numbers.

Category

Chemical class: Monomethanesulfonate, nonbiphenyl nontetrazole angiotensin II receptor antagonist
Therapeutic class: Antihypertensive

Pregnancy category: Not rated

Indications

To control blood pressure in patients with essential hypertension
Adults. Initial: 600 mg daily. Maximum: 800 mg once daily or in divided doses b.i.d.

Mechanism of Action

Blocks the effects of angiotensin II (a potent vasoconstrictor that’s part of the renin-angiotensin-aldosterone system) by blocking its binding to angiotensin I receptors in vascular smooth muscles, adrenal glands, and other tissues. This action halts angiotensin II’s negative feedback on renin secretion. Thus, circulating renin and angiotensin II levels rise and vascular resistance declines.

Contraindications

Hypersensitivity to eprosartan or components

Side Efect

CNS: Depression, dizziness, drowsiness, fatigue
CV: Angina pectoris, atrial fibrillation, bradycardia, extrasystole, hypertriglyceridemia, hypotension, palpitations, tachycardia
EENT: Pharyngitis, rhinitis
GI: Abdominal pain
GU: Oliguria, UTI
MS: Myalgia, rhabdomyolysis
RESP: Cough, upper respiratory tract infection

Cautions

Watch for excessive hypotension if patient receives other cardiac .

Expect maximum blood pressure response after about 3 weeks.

Be aware that, unlike ACE inhibitors, eprosartan doesn’t affect bradykinin breakdown and cause the characteristic ACE cough.

PATIENT SAFTY

Explain that maximum blood pressure response may not occur for 3 to 4 weeks.

Tell patient that drug may cause dizziness, drowsiness, or very low blood pressure. Urge him to rise slowly to upright position.

Category

Chemical class: Cyclic heptapeptide
Therapeutic class: Platelet aggregation inhibitor

Pregnancy category: B

eprosartan mesylate;eptifibatide 381 E F

Indications

To treat unstable angina and non–Qwave MI
IV:
Adults. Initial: 180 mcg/kg over 1 to 2 min as soon as possible after diagnosis. Maintenance: 2 mcg/kg/min by continuous infusion starting immediately after initial dose and continuing until discharge or coronary artery bypass grafting, up to 72 hr.
DOSAGE ADJUSTMENT For patients with serum creatinine level of 2 to 4 mg/dl, initial dosage reduced to 135 mcg/kg over 1 to 2 min and maintenance dosage to 0.5 mcg/ kg/min by continuous infusion. Dosage discontinued before coronary artery bypass graft surgery or if platelet count is less than 100,000/mm3. To prevent thrombosis related to percutaneous transluminal coronary angioplasty (PTCA)
IV:
Adults.Initial: 135 mcg/kg over 1 to 2 min immediately before procedure. Maintenance: 0.5 mcg/kg/min by continuous infusion beginning just after initial dose and continuing for 20 to 24 hr. Maximum: 96 hr of therapy. Route Onset Peak Duration I.V. Immediate In 15 min 4–8 hr

Mechanism of Action

Reversibly inhibits platelet aggregation by preventing fibrinogen, von Willebrand factor, and other adhesive ligands from binding to glycoprotein IIb/IIIa receptors on activated platelets. As a result, eptifibatide disrupts final cross-linking stage of platelet aggregation—and thrombus formation.

Incompatibilities

Don’t administer eptifibatide through the same I.V. line as furosemide.

Contraindications

Active bleeding or stroke during prior 30 days, bleeding diathesis, dependency on dialysis, history of hemorrhagic stroke, hypersensitivity to eptifibatide, major surgery during previous 4 weeks, serum creatinine level of 2 mg/dl or higher (for 180mcg/kg dose or 2-mcg/kg/min infusion) or 4 mg/dl or higher (for 135-mcg/kg dose or 0.5-mcg/kg/min infusion), severe uncontrolled hypertension (systolic pressure above 200 mm Hg, diastolic pressure above 110 mm Hg), thrombocytopenia (platelet count below 100,000/mm3)

Interactions

anticoagulants, clopidogrel, dipyridamole, NSAIDs, thrombolytics, ticlopidine: Additive pharmacologic effects, increased risk of bleeding other platelet aggregation inhibitors (especially inhibitors of platelet receptor glycoprotein IIb/IIIa, such as abciximab): Increased risk of additive pharmacologic effects

Side Efect

CNS: Intracranial hemorrhage
CV: Hypotension
GI: Hematemesis
GU: Hematuria
HEME: Bleeding, decreased hemoglobin level, thrombocytopenia
Other: Anaphylaxis

Cautions

Expect to obtain APTT and PT as a baseline and hematocrit, platelet count, and hemoglobin and serum creatinine levels before therapy.

Withdraw bolus dose of eptifibatide from a 10-ml (2 mg/ml) vial into a syringe.

Using vented I.V. infusion set, give continuous infusion directly from the 100-ml (0.75 mg/ml) vial. Be sure to center the spike in the circle on top of vial stopper.

Expect to keep APTT between 50 and 70 seconds or per facility protocol during therapy unless patient has PTCA.

If patient has PTCA, expect to maintain activated clotting time between 200 and 250 seconds during the procedure.

During therapy, avoid arterial and venous punctures, I.M. injections, urinary catheters, nasotracheal or nasogastric intubation, and use of noncompressible I.V. sites, such as subclavian and jugular veins.

Expect to discontinue eptifibatide and heparin and monitor patient closely if platelet count falls below 100,000/mm3.

Plan to stop drug, as prescribed, if patient undergoes coronary artery bypass surgery.

PATIENT SAFTY

Instruct patient to immediately report bleeding during eptifibatide therapy.

Reassure patient that he’ll be monitored closely throughout therapy.

Advise patient to avoid activities that may lead to bruising and bleeding.

Category

Chemical class: Dihydrogenated ergot alkaloid derivative
Therapeutic class: Antidementia adjunct, cerebral metabolic enhancer

Pregnancy category: Not rated

Indications

To treat age-related decline in mental capacity ,, S.L.,
Adults. 1 to 2 mg t.i.d. Route Onset Peak Duration P.O. 3 wk Unknown Unknown or more

Mechanism of Action

May increase cerebral metabolism, blood flow, and oxygen uptake. These actions may increase neurotransmitter levels.

Contraindications

Acute or chronic psychosis, hypersensitivity to ergoloid mesylates or their components

Interactions

delavirdine, efavirenz, indinavir, nelfinavir, saquinavir: Increased risk of ergotism (blurred vision, dizziness, and headache) dopamine: Increased risk of gangrene

Side Efect

CNS: Dizziness, headache, light-headedness, syncope
CV: Bradycardia, orthostatic hypotension
EENT: Blurred vision, nasal congestion, tongue soreness (with S.L. tablets)
GI: Abdominal cramps, anorexia, nausea, vomiting
SKIN: Flushing, rash

Cautions

Expect ergoloid mesylates to be prescribed only after a pathophysiologic cause for mental decline has been ruled out.

Measure blood pressure and pulse rate and rhythm before therapy begins and monitor them frequently during therapy.

If bradycardia or hypotension develops, expect to discontinue drug permanently.

PATIENT SAFTY

Stress the importance of adhering to prescribed dosage and schedule.

Teach caregiver to place S.L. tablet under patient’s tongue and withhold food, fluids, and cigarettes until tablet dissolves.

Instruct patient not to swallow S.L. tablets.

Advise caregiver to skip a missed dose and resume the regular dosing schedule. Warn against doubling the dose, and urge caregiver to notify prescriber if patient misses two or more doses in a row.

Instruct caregiver to store drug in a tightly closed, light-resistant container.

Inform caregiver and family that drug may take 3 to 4 weeks to produce its effects.

Stress the importance of follow-up care.

Category

Chemical class: Ergot alkaloid
Therapeutic class: Vascular headache suppressant

Pregnancy category: X

Indications

To relieve vascular headaches, such as migraine, migraine variants, and cluster headaches S.L.
Adults. Initial: 2 mg at first sign of attack and repeated every 30 min, p.r.n. Maximum: 6 mg/day and no more than twice/wk at least 5 days apart.
Adults. Initial: 1 to 2 mg at first sign of attack, repeated every 30 min, p.r.n. Increased to 3 mg for subsequent attacks if needed and if lower dose was well tolerated. Maximum: 6 mg daily. ORAL INHALATION AEROSOL
Adults.1 (360-mcg) inhalation at first sign of attack and repeated every 5 min, p.r.n. ergoloid mesylates;ergotamine tartrate 383 E F Maximum: 2.16 mg daily and no more than twice/wk at least 5 days apart. Route Onset Peak Duration P.O., S.L. Unknown 1–5 hr Unknown

Mechanism of Action

Directly stimulates vascular smooth muscles, constricting arteries and veins and depressing vasomotor centers in the brain.

Contraindications

Coronary artery disease, hypersensitivity to ergot alkaloids, hypertension, impaired hepatic or renal function, malnutrition, peripheral vascular disease (Raynaud’s disease, severe arteriosclerosis, syphilitic arteritis, thromboangiitis obliterans, thrombophlebitis), pregnancy or risk of pregnancy, sepsis, severe pruritus

Interactions

beta blockers: Increased risk of vasoconstriction and, possibly, peripheral gangrene erythromycin, troleandomycin: Possibly increased risk of peripheral vasospasm and ischemia nitrates: Increased ergotamine effects, decreased antianginal effects of nitrates, increased risk of hypertension sumatriptan: Possibly additive vasoconstriction vasoconstrictors: Increased risk of dangerous hypertension smoking: Possibly increased risk of peripheral vasoconstriction and ischemia

Side Efect

CNS: Anxiety, confusion, dizziness, drowsiness, paresthesia, severe headache
CV: Chest pain, fast or slow heart rate, heart valve fibrosis, increased or decreased blood pressure, MI, weak pulse
EENT: Dry mouth, miosis, vision changes
GI: Nausea, vomiting
MS: Arm, back, or leg pain; muscle weakness in legs
SKIN: Cold, cyanotic, or pale feet or hands; pruritus
Other: Edema of face, feet, fingers, or lower legs; physical dependence

Cautions

Use ergotamine cautiously in elderly patients.

If patient receives long-term therapy, monitor pain control; he may need increasingly higher doses to obtain relief.

Notify prescriber at the first sign of vasospasm and expect to discontinue drug.

PATIENT SAFTY

Teach patient to take a tablet at the first sign of headache and to lie down in a quiet, dark room.

Instruct patient not to swallow S.L. tablet but to let it dissolve under his tongue. Advise him not to drink, eat, or smoke until tablet has dissolved.

Stress the importance of adhering to prescribed dosage and schedule because of drug’s potential for dependence.

Warn patient not to smoke while taking ergotamine (especially heavy smokers) because combining drug with nicotine, which also constricts vessels, may increase risk of peripheral vascular ischemia.

Advise patient to notify prescriber if usual doses fail to relieve headaches or if headache frequency or severity increases.

Urge patient to avoid alcohol because it worsens headaches. Also suggest that patient avoid excessive cold, which may increase peripheral vasoconstriction.

Instruct patient to notify prescriber if an infection develops because severe infection may increase sensitivity to drug.

Advise patient to notify prescriber if he experiences chest pain; numbness, pain, or tingling in fingers or toes; pulse rate changes; swelling of face, feet, fingers, or lower legs; or vision changes.

Category

Chemical class: Synthetic 1-b methylcarbapenem
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat moderate to severe infections, such as complicated intra-abdominal infections due to Escherichia coli, Clostridium clostridioforme, Eubacterium lentum, Pepto-streptoertapenem sodium 384 coccus species, Bacteroides fragilis, B. distasonis, B. ovatus, B. thetaiotaomicron, or B. uniformis; complicated skin and skin-structure infections due to Staphylococcus aureus (methicillinsusceptible strains only), Streptococcus pyogenes, E. coli, or Peptostreptococcus species; community-acquired pneumonia due to Streptococcus pneumoniae (penicillin-susceptible strains only, including cases with concurrent bacteremia), Haemophilus influenzae (beta-lactamase–negative strains only), or Moraxella catarrhalis; complicated UTI (including pyelonephritis) due to E. coli (including cases with concurrent bacteremia) or Klebsiella pneumoniae; and acute pelvic infections (including postpartum endomyometritis, septic abortion, and postsurgical gynecologic infections) due to Streptococcus agalactiae, E. coli, B. fragilis, Porphyromonas asaccharolytica, Peptostreptococcus species, or Prevotella bivia

IV

Adults and adolescents. 1 g daily, infused over 30 min, for up to 14 days. Children ages 3 months to 13 years.15 mg/ kg b.i.d., infused over 30 min, for up to 14 days. Maximum: 1 g daily.

IM

Adults and adolescents.1 g daily for up to 7 days. Children ages 3 months to 13 years. 15 mg/ kg b.i.d. for up to 7 days. Maximum: 1 g daily.
DOSAGE ADJUSTMENT Dosage decreased to 500 mg daily for patients with advanced renal insufficiency (creatinine clearance less than or equal to 30 ml/min/1.73 m2) or end-stage renal insufficiency (creatinine clearance less than or equal to 10 ml/min/ 1.73 m2). For patients on hemodialysis who have received 500 mg of ertapenem within 6 hr of hemodialysis, supplemental dose of 150 mg given after hemodialysis.

Mechanism of Action

Inhibits bacterial cell wall synthesis by binding to specific penicillin-binding proteins inside the cell wall. Penicillin-binding proteins are responsible for various steps in bacterial cell wall synthesis. By binding to these proteins, ertapenem leads to bacterial cell wall lysis.

Incompatibilities

Don’t mix ertapenem with other . Don’t dilute it with solutions containing dextrose.

Contraindications

Hypersensitivity to ertapenem, its components, or other in the same class; hypersensitivity to local anesthetics (I.M. form only, because lidocaine hydrochloride 1% is used as a diluent); patients who have experienced anaphylactic reactions to betalactam

Interactions

probenecid: Increased ertapenem half-life, increased and prolonged blood ertapenem level
valproic acid: Possibly decreased serum valproic acid level and increased risk of breakthrough seizures

Side Efect

CNS: Aggression, agitation, anxiety, asthenia, confusion, delirium, disorientation, dizziness, dyskinesia, fatigue, fever, hallucinations, headache, hypothermia, insomnia, mental changes, myoclonus, seizures, somnolence, stupor, tremor
CV: Chest pain, edema, hypertension, hypotension, tachycardia, thrombophlebitis
EENT: Nasopharyngitis, oral candidiasis, viral pharyngitis
ENDO: Hyperglycemia
GI: Abdominal pain, acid regurgitation, Clostridium difficile colitis, constipation, diarrhea, elevated liver function test results, indigestion, nausea, small-intestine obstruction, vomiting
GU: Dysuria, elevated serum creatinine level, proteinuria, RBCs and WBCs in urine, UTI, vaginitis
HEME: Anemia, decreased hematocrit, decreased WBC count, eosinophilia, increased WBC count, neutropenia, prolonged PT, thrombocytopenia, thrombocytosis
MS: Leg pain
RESP: Atelectasis, cough, crackles, dyspnea, pneumonia, respiratory distress, upper respiratory tract infection, wheezing
SKIN: Cellulitis, dermatitis, erythema, extravasation, pruritus, rash
Other: Anaphylaxis; death; hyperkalemia; hypokalemia; infusion site induration, pain, ertapenem sodium 385 E F phlebitis, redness, swelling, or warmth

Cautions

Obtain sputum, urine, or other specimens for culture and sensitivity testing, as ordered, before giving ertapenem. Expect to start therapy before results are available.

When preparing drug for I.V. use, reconstitute 1 g with 10 ml of sterile water for injection, 0.9% sodium chloride injection, or bacteriostatic water for injection. Don’t use solutions that contain dextrose. Shake well to dissolve. Immediately transfer reconstituted drug to 50 ml normal saline solution. Use within 6 hours if stored at room temperature, 24 hours if refrigerated at 5° C (41° F). Don’t freeze. Give I.V. infusion over 30 minutes.

Inspect drug for particles and discoloration after reconstitution.

For I.M. injection, reconstitute 1 g of drug with 3.2 ml of 1% lidocaine hydrochloride injection (without epinephrine). Shake thoroughly to form solution. Use within 1 hour after preparation. Withdraw contents of vial and inject deep into a large muscle mass such as the gluteal muscle.
WARNING Don’t give reconstituted I.M. solution by I.V. route because of possible adverse reaction to lidocaine hydrochloride injection used to reconstitute drug.

Monitor patient closely for a life-threatening anaphylactic reaction. Patients with a history of hypersensitivity to penicillin, cephalosporins, other beta-lactams, or other allergens are at increased risk.
WARNING If ertapenem triggers an anaphylactic reaction, stop drug, notify prescriber immediately, and provide appropriate therapy. Anaphylaxis requires immediate treatment with epinephrine as well as airway management and administration of oxygen and I.V. corticosteroids, as needed.

Be aware that patients with a history of seizures, other CNS disorders that predispose them to seizures (such as brain lesions), or compromised renal function may be at increased risk for seizures. Administer anticonvulsant, as ordered.

Monitor patient for diarrhea during and for at least 2 months after drug therapy; diarrhea may signal pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold ertapenem and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Be aware that because ertapenem is excreted in breast milk, its use by nursing mothers is carefully evaluated.

PATIENT SAFTY

Instruct patient receiving ertapenem to immediately report signs of anaphylaxis, such as rash, itching, or shortness of breath; or signs of superinfection, such as severe diarrhea or white patches on tongue or in mouth.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and can be serious, requiring prompt treatment.

Category

Chemical class: Macrolide
Therapeutic class: Antiacne agent, antibiotic

Pregnancy category: B

Indications

To treat mild to moderate upper respiratory tract infections caused by Haemophilus influenzae, Streptococcus pneumoniae, or Streptococcus pyogenes (group A betahemolytic streptococcus) , CHEWABLE , DELAYED-RELEASE , DELAYED-RELEASE , ORAL SUSPENSION,,
IV:
Adults. 250 to 500 mg (base) every 6 hr for 10 days. Children.250 to 500 mg (base) q.i.d. or 20 to 50 mg (base)/kg daily in divided doses for 10 days. For H. influenzae infections, erythromycin ethylsuccinate is administered with 150 mg/kg daily of sulfisoxazole. Maximum: Adult dosage, or 6 g daily for erythromycin ethylsuccinate. To treat lower respiratory tract infections caused by S. pneumoniae or S. pyogenes (group A beta-hemolytic streptococcus) , CHEWABLE , DELAYED-RELEASE , DELAYED-RELEASE , ORAL SUSPENSION,,
IV:
Adults.250 to 500 mg (base) every 6 hr for 10 days. Children.250 to 500 mg (base) q.i.d. or 20 to 50 mg (base)/kg daily in divided doses for 10 days. Maximum: Adult dosage. To treat respiratory tract infections caused by Mycoplasma pneumoniae , CHEWABLE , DELAYED-RELEASE , DELAYED-RELEASE , ORAL SUSPENSION,,
IV:
Adults.500 mg (base) every 6 hr for 5 to 10 days or up to 3 wk for severe infections. To treat mild to moderate skin and softtissue infections caused by S. pyogenes or Staphylococcus aureus , CHEWABLE , DELAYED-RELEASE , DELAYED-RELEASE , ORAL SUSPENSION,,
IV:
Adults. 250 mg (base) every 6 hr or 500 mg (base) every 12 hr for 10 days. Maximum: 4 g (base) daily. Children. 250 to 500 mg (base) q.i.d. or 20 to 50 mg (base)/kg daily in divided doses for 10 days. Maximum: Adult dosage. To treat acne vulgaris DELAYED-RELEASE , DELAYED-RELEASE , Adults and adolescents. Initial: 250 mg (base) every 6 hr, 333 mg (base) every 8 hr, or 500 mg (base) every 12 hr for 4 wk. Maintenance: 333 to 500 mg (base) daily. To treat pertussis (whooping cough) caused by Bordetella pertussis , CHEWABLE , DELAYED-RELEASE , DELAYED-RELEASE , ORAL SUSPENSION,,
IV: Children.500 mg (base) q.i.d. or 40 to 50 mg (base)/kg daily in divided doses for 5 to 14 days. To treat diphtheria , CHEWABLE , DELAYED-RELEASE , DELAYED-RELEASE , ORAL SUSPENSION,,
IV: Adults and children.500 mg (base) every 6 hr for 10 days. To treat erythrasma , CHEWABLE , DELAYED-RELEASE , DELAYED-RELEASE , ORAL SUSPENSION,,
IV: Adults and children.250 mg (base) t.i.d. for 21 days. To treat intestinal amebiasis , CHEWABLE , DELAYED-RELEASE , DELAYED-RELEASE , ORAL SUSPENSION,,
IV:
Adults.250 mg (base) every 6 hr for 10 to 14 days. Children. 30 to 50 mg (base)/kg daily in erythromycin 387 E F divided doses for 10 to 14 days To treat pelvic inflammatory disease caused by Neisseria gonorrhoeae , CHEWABLE , DELAYED-RELEASE , DELAYED-RELEASE , ORAL SUSPENSION,,
IV:
Adults.500 mg (base) I.V. every 6 hr for 3 days and then 250 mg (base) P.O. or I.V. every 6 hr for 7 days. To treat conjunctivitis in newborns
IV: Neonates.50 mg (base)/kg daily in 4 divided doses for 14 days. To treat pneumonia in neonates
IV: Neonates.50 mg (base)/kg daily in divided doses for 21 days. To treat urogenital infections caused by Chlamydia trachomatis during pregnancy ,CHEWABLE ,DELAYED-RELEASE ,DELAYED-RELEASE , ORAL SUSPENSION,
Adults. 500 mg (base) on an empty stomach every 6 hr for 7 days; or 250 mg (base) on an empty stomach every 6 hr for at least 14 days. To treat nongonococcal urethritis or uncomplicated urethral, endocervical, or rectal infections caused by C. trachomatis , CHEWABLE , DELAYED-RELEASE , DELAYED-RELEASE , ORAL SUSPENSION,
Adults.500 mg (base) every 6 hr for 7 days. If patient can’t tolerate high doses, 250 mg (base) every 6 hr for 14 days. To treat primary syphilis ,CHEWABLE ,DELAYED-RELEASE ,DELAYED-RELEASE , ORAL SUSPENSION,
Adults. 20 to 40 g (base) in divided doses over 10 to 15 days. To treat Legionnaire’s disease , CHEWABLE , DELAYED-RELEASE , DELAYED-RELEASE , ORAL SUSPENSION,,
IV:
Adults.1 to 4 g (base) daily in divided doses for 10 to 14 days. To treat rheumatic fever , CHEWABLE , DELAYED-RELEASE , DELAYED-RELEASE , ORAL SUSPENSION, ,

IV

Adults.250 mg (base) every 12 hr. To prevent bacterial endocarditis in patients with penicillin allergy who plan dental or upper respiratory tract surgery , CHEWABLE , DELAYED-RELEASE , DELAYED-RELEASE , ORAL SUSPENSION, ,

IV

Adults.1 g (base) given 1 to 2 hr before procedure and then 500 mg (base) 6 hr after initial dose. Children.20 mg (base)/kg given 2 hr before procedure and then 10 mg (base)/kg 6 hr after initial dose. To treat listeriosis , CHEWABLE , DELAYED-RELEASE , DELAYED-RELEASE , ORAL SUSPENSION,,
IV:
Adults.250 mg (base) every 6 hr or 500 mg (base) every 12 hr. Maximum: 4 g (base) daily.

Mechanism of Action

Binds with the 50S ribosomal subunit of the 70S ribosome in many types of aerobic, anaerobic, gram-positive, and gram-negative bacteria. This action inhibits RNAdependent protein synthesis in bacterial cells, causing them to die.

Contraindications

Astemizole, cisapride, pimozide, or terfenadine therapy; hypersensitivity to erythromycin, macrolide antibiotics, or their components; hepatic disease (erythromycin estolate)

Interactions

alfentanil: Decreased alfentanil clearance, prolonged alfentanil action astemizole, cisapride, terfenadine: Increased risk of cardiotoxicity, torsades de pointes, ventricular tachycardia, and death atorvastatin, lovastatin, pravastatin, simvastatin: Increased risk of rhabdomyolysis carbamazepine,
valproic acid: Possibly inhibited metabolism of these , increasing their blood levels and risk of toxicity chloramphenicol, lincomycins: Antagonized effects of these cyclosporine: Increased risk of nephrotoxicity digoxin: Increased serum digoxin level and risk of digitalis toxicity diltiazem, verapamil: Increased risk of lifethreatening cardiac events ergotamine: Decreased ergotamine metabolism, increased risk of vasospasm from erythromycin 388 ergotamine use hepatotoxic : Increased risk of hepatotoxicity midazolam, triazolam: Increased pharmacologic effects of these oral contraceptives: Failed contraception, hepatotoxicity ototoxic : Increased risk of ototoxicity if patient with impaired renal function receives high doses of erythromycin penicillins: Interference with bactericidal effects of penicillins
sildenafil: Increased effects of sildenafil
warfarin: Prolonged PT and risk of hemorrhage, especially in elderly patients xanthines (except dyphylline): Increased serum theophylline level and risk of theophylline toxicity
alcohol use: Increased alcohol level (by 40%) with I.V. erythromycin

Side Efect

CNS: Fatigue, fever, malaise, weakness
CV: Prolonged QT interval, torsades de pointes, ventricular arrhythmias
EENT: Hearing loss, oral candidiasis
GI: Abdominal cramps and pain, diarrhea, hepatotoxicity, nausea, pseudomembranous colitis, vomiting
GU: Vaginal candidiasis
MS: New or aggravated myasthenia gravis syndrome
SKIN: Erythema, jaundice, pruritus, rash
Other: Fluid overload (from I.V. infusion), injection site inflammation and phlebitis

Cautions

Use erythromycin cautiously in patients with impaired hepatic function because drug is metabolized by the liver.

Use erythromycin cautiously in elderly patients, especially those with renal or hepatic dysfunction, because these patients are at increased risk of hearing loss and torsades de pointes. They’re also at increased risk of bleeding if taking an oral anticoagulant.

Before giving first erythromycin dose, expect to obtain body fluid or tissue sample for culture and sensitivity testing.

Reconstitute parenteral form before administration. Add at least 10 ml of preservative-free sterile water for injection to each 500-mg vial or at least 20 ml of diluent to each 1-g vial.

For prolonged infusion, expect to infuse a buffered solution up to 24 hours after dilution.

For intermittent infusion, dilute dose in 100 to 250 ml normal saline solution or D5W if needed; give slowly over 20 to 60 minutes.

When giving I.V. erythromycin gluceptate, dilute the solution if needed to 1 g/L in normal saline solution or D5W injection for slow, continuous infusion. Diluted solution remains potent for 7 days if refrigerated.

When giving I.V. erythromycin lactobionate, dilute the solution if needed to 1 to 5 mg/ml in normal saline solution, lactated Ringer’s solution, or other electrolyte solution for slow, continuous infusion. Diluted solution remains potent for 14 days if refrigerated and for 24 hours at room temperature.

Be aware that infusions prepared in piggyback infusion bottles stay potent for 30 days if frozen, 24 hours if refrigerated, or 8 hours at room temperature. Don’t store infusions prepared in the ADDvantage system.

Don’t use diluent with benzyl alcohol if parenteral erythromycin is for a neonate. It may cause a fatal toxic syndrome of CNS depression, hypotension, metabolic acidosis, renal failure, respiratory problems, and, possibly, seizures and intracranial hemorrhage.

Periodically monitor liver function test results to detect hepatotoxicity, which is most common with erythromycin estolate. Signs typically appear within 2 weeks after continuous therapy starts and resolve when it stops.

Assess hearing regularly, especially in elderly patients and those who receive 4 g or more daily or have hepatic or renal disease. Hearing impairment begins 36 hours to 8 days after treatment starts and usually begins to improve 1 to 14 days after it stops.

During I.V. therapy, watch for evidence of fluid overload, such as acute dyspnea and crackles.

Monitor infants for vomiting or irritability with feeding because infantile hypertrophic pyloric stenosis has been reported. erythromycin 389 E F

Assess myasthenia gravis patients for weakness because drug may aggravate it. Keep in mind that myasthenic syndrome may arise in patients previously undiagnosed with myasthenia gravis.

Watch closely for signs and symptoms of superinfection. If they occur, notify prescriber and expect to stop drug and provide appropriate therapy.

Monitor patient for diarrhea during and for at least 2 months after erythromycin therapy; diarrhea may signal pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold drug and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

If patient receives an order for urine catecholamine analysis, notify prescriber because erythromycin interferes with fluorometric measurement of urine catecholamines.

PATIENT SAFTY

Urge patient to complete prescribed therapy, even if he feels better before it’s finished.

Tell patient to notify prescriber if symptoms worsen or don’t improve after a few days.

Teach patient how to administer prescribed form of erythromycin. Instruct him to swallow capsules or tablets whole. For an oral suspension, teach him to use the calibrated measuring device provided to ensure accurate doses. Remind him to shake the suspension before measuring a dose.

Advise patient to take oral form of erythromycin with a full glass of water on an empty stomach (except erythromycin ethylsuccinate, which is better absorbed with food).

If GI distress occurs, instruct patient to take oral form with food.

Instruct patient to promptly notify prescriber if he develops allergic reactions, hearing changes, or signs of hepatic dysfunction.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and can be serious, requiring prompt treatment.

Category

Chemical class: Pure S1 enantiomer of racemic bicyclic phthalane derivative citalopram
Therapeutic class: Antidepressant

Pregnancy category: C

Indications

To treat generalized anxiety disorder or major depression

ORALL

,
Adults.Initial: 10 mg daily in morning or evening, increased to 20 mg daily after 1 or more wk, as needed. To treat major depression

ORALL

,
Adults. Initial: 10 mg daily, morning or evening, increased to 20 mg daily after 1 wk, as needed. Adolescents ages 12 to 17. Initial: 10 mg daily, morning or evening, increased to 20 mg daily after 3 wk, as needed.
DOSAGE ADJUSTMENT Dosage shouldn’t exceed 10 mg daily for elderly patients and those with hepatic impairment.

Mechanism of Action

Inhibits reuptake of the neurotransmitter serotonin by CNS neurons, thereby increasing the amount of serotonin available in nerve synapses. An elevated serotonin level may result in elevated mood and reduced depression.

Contraindications

Hypersensitivity to escitalopram, citalopram or its components; use within 14 days of MAO inhibitor therapy

Interactions

aspirin, NSAIDs,
warfarin: Possibly increased risk of bleeding carbamazepine: Possibly increased clearance of escitalopram
cimetidine: Possibly increased plasma escitalopram level CNS : Additive CNS effects lithium: Possible enhancement of the seroescitalopram oxalate 390 tonergic effects of escitalopram
MAO inhibitors: Possibly hyperpyretic episodes, hypertensive crisis, serotonin syndrome, and severe seizures metoprolol: Increased plasma metoprolol levels with decreased cardioselectivity of metoprolol naratriptan, sumatriptan, zolmitriptan: Possibly weakness, hyperreflexia, and incoordination
St. John’s wort: Increased risk of serotonin syndrome sibutramine: Increased risk of serotonin syndrome
alcohol use: Possibly increased cognitive and motor effects of alcohol

Side Efect

CNS: Abnormal gait, acute psychosis, aggression, akathisia, delirium, dizziness, dyskinesia, dystonia, extrapyramidal effects, fatigue, headache, hypomania, insomnia, lethargy, mania, myoclonus, neuroleptic malignant syndrome, paresthesia, seizures, serotonin syndrome, somnolence, suicidal ideation
CV: Atrial fibrillation, cardiac failure, deep vein or phlebitis thrombosis, hypotension, MI, prolonged QT interval, thrombosis, torsades de pointes, ventricular arrhythmias
EENT: Diplopia, dry mouth, glaucoma, nystagmus, rhinitis, sinusitis, toothache, visual hallucinations
ENDO: Diabetes mellitus, hyperprolactinemia, syndrome of inappropriate ADH secretion
GI: Abdominal pain, constipation, decreased appetite, diarrhea, flatulence, GI bleeding or hemorrhage, hepatic necrosis, hepatitis, indigestion, nausea, pancreatitis, rectal hemorrhage, vomiting
GU: Acute renal failure, anorgasmia, decreased libido, ejaculation disorders, impotence, priapism
HEME: Bleeding, decreased prothrombin time, hemolytic anemia, leukopenia, thrombocytopenia
MS: Neck or shoulder pain, rhabdomyolysis
RESP: Pulmonary embolism
SKIN: Ecchymosis, erythema multiforme, increased sweating, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, flulike symptoms, hyponatremia

Cautions

Use escitalopram cautiously in patients with history of mania or seizures, patients with severe renal impairment, and those with diseases or conditions that produce altered metabolism or hemodynamic responses.

Monitor patient—especially elderly patient—for hypoosmolarity of serum and urine and for hyponatremia (headache, trouble contentrating, impaired memory, weakness, unsteadiness) because they may may indicate escitalopram-induced syndrome of inappropriate ADH secretion.

Watch for signs of misuse or abuse, such as development of tolerance, increasing dosage without approval, and drug-seeking behavior; drug’s potential for physical and psychological dependence is unknown.

Monitor patient for bleeding, especially if patient is also taking aspirin, an NSAID, or an anticoagulant. Bleeding can range from ecchymoses, hemtomas, epitaxis and petechiae to life-threatening hemorrhages.

Expect prescriber to reassess patient periodically to determine the continued need for therapy and evaluate dosage.

If patient (particularly a child or an adolescent) takes escitalopram for depression, watch closely for suicidal tendencies, especially when therapy starts or dosage changes, because depression may worsen temporarily.

If escitalopram will be stopped, expect to taper dosage to avoid serious adverse reactions.

PATIENT SAFTY

Inform patient that alcohol use isn’t recommended during escitalopram therapy because it may decrease his ability to think clearly and perform motor skills.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient that drug shouldn’t be taken with citalopram hydrobromide because of potentially additive effects.

Tell patient that improvement may not be noticed for 1 to 4 weeks after therapy begins. Emphasize the importance of continuing therapy as prescribed.

If patient (particularly a child or an adolescent) takes drug for depression, urge escitalopram oxalate 391 E F caregivers to watch closely for suicidal tendencies, especially when therapy starts or dosage changes.

Warn patient not to stop taking drug abruptly. Explain that gradual tapering helps to avoid withdrawal symptoms.

Urge patient to inform prescriber of any OTC he takes because of potential for interactions.

Review signs and symptoms of hyponatremia, and instruct patient to report them to prescriber.

Warn patient that escitalopram increases bleeding risk if taken with aspirin, an NSAID, or an anticoagulants and that bleeding events could range from mild to severe. Tell patient to seek emergency care for serious or prolonged bleeding.

Category

Chemical class: Beta blocker
Therapeutic class: Antiarrhythmic, antihypertensive

Pregnancy category: C

Indications

To treat supraventricular tachycardia
IV:
Adults.Loading: 500 mcg/kg over 1 min. Maintenance: If response to loading dose is adequate after 5 min, 50 mcg/kg/min infused for 4 min. If response is inadequate after 5 min, another 500 mcg/kg may be given over 1 min followed by 100 mcg/kg/ min for 4 min. Sequence repeated, as needed, until adequate response occurs, increasing maintenance dosage by 50 mcg/kg/min at each step. Maximum: 200 mcg/kg/min for 48 hr. Children. 50 mcg/kg/min titrated every 10 min up to 300 mcg/kg/min. To treat intraoperative and postoperative tachycardia and hypertension
IV:
Adults.Initial: 250 to 500 mcg/kg over 1 min. Maintenance: 50 mcg/kg/min infused over 4 min. If response is inadequate after 5 min, another 250 to 500 mcg/ kg may be given over 1 min followed by 100 mcg/kg/ min for 4 min. Sequence repeated, as needed, up to 4 times, increasing by 50 mcg/kg/min each time. Maximum: 200 mcg/kg/min for 48 hr.
DOSAGE ADJUSTMENT Loading doses omitted, increments decreased to 25 mcg/kg/ min, and titration intervals increased to 10 min as heart rate approaches desired level or if blood pressure decreases too much. Route Onset Peak Duration I.V. Immediate Unknown 10–20 min

Mechanism of Action

Inhibits stimulation of beta1receptors mainly in the heart, which decreases cardiac excitability, cardiac output, and myocardial oxygen demand. Esmolol also decreases renin release from kidneys, which helps reduce blood pressure.

Incompatibilities

Don’t mix esmolol with 5% sodium bicarbonate injection.

Contraindications

Cardiogenic shock, hypersensitivity to beta blockers, overt heart failure, secondor third-degree heart block, sinus bradycardia

Interactions

antihypertensives: Possibly hypotension insulin, oral antidiabetics: Possibly masking of signs and symptoms of hypoglycemia caused by these
MAO inhibitors: Possibly severe hypertension if esmolol is given within 14 days of discontinuing MAO inhibitor therapy neuromuscular blockers: Possibly potentiated and prolonged action of these
phenytoin: Possibly increased cardiac depression reserpine: Possibly bradycardia and hypotension sympathomimetics, xanthine derivatives: Possibly inhibited therapeutic effects of both

Side Efect

CNS: Anxiety, confusion, depression, dizziness, fatigue, fever, headache, syncope
CV: Bradycardia, chest pain, decreased peripheral circulation, heart block, esmolol hydrochloride 392 hypotension
GI: Nausea, vomiting
RESP: Dyspnea, wheezing
SKIN: Diaphoresis, flushing, pallor
Other: Infusion site pain, redness, and swelling

Cautions

Use esmolol cautiously if patient has supraventricular arrhythmias with decreased cardiac output, hypotension, or other hemodynamic compromise or is taking that decrease peripheral resistance or myocardial filling, contractility, or impulse generation.

Also use drug cautiously in patients with impaired renal function because drug is excreted by the kidneys. Patients with endstage renal disease have an increased risk of

Side Efect

.

Avoid giving esmolol for intraoperative or postoperative hypertension caused by hypothermia-induced vasoconstriction.

Expect to give lowest possible dose to patients with allergies, asthma, bronchitis, or emphysema. If patient develops broncho-spasm, expect to discontinue infusion immediately and give a beta2-stimulating drug, as ordered.

Don’t give 250 mg/ml (2,500 mg/10 ml) dosage strength by direct I.V. push. Dilute it to a 10-mg/ml infusion by first removing 20 ml from 500 ml of a compatible I.V. solution, such as D5W or dextrose 5% in normal saline solution, and then adding 5 g of esmolol to the solution.

Use diluted solution within 24 hours if stored at room temperature.

Use 100-mg vial (prediluted to 10 mg/ml) for loading dose. For 70-kg (154-lb) patient, loading dose for 500 mcg/kg/min is 3.5 ml.

Monitor blood pressure and heart rate often during therapy. Hypotension can occur at any dose but usually is dose related. It typically reverses within 30 minutes after dose is decreased or infusion stopped.

Inspect site often for thrombophlebitis (pain, redness, swelling at site). Infusion of 20 mg/ml is more likely to cause serious vein irritation than 10 mg/ml. Extravasation of 20 mg/ml may cause a serious local reaction and skin necrosis. Don’t give more than 10 mg/ml into a small vein or using a butterfly catheter.

PATIENT SAFTY

Urge patient to report

Side Efect

immediately.

Reassure patient that his blood pressure, heart rate, and response to therapy will be monitored throughout esmolol therapy.

Category

Chemical class: Substituted benzimidazole
Therapeutic class: Antiulcerative

Pregnancy category: B

Indications

To treat gastroesophageal reflux disease (GERD) DELAYED-RELEASE
Adults. 20 to 40 mg daily for 4 to 8 wk; may be repeated for another 4 to 8 wk if ulcer hasn’t healed. Maintenance: 20 mg daily for up to 6 mo. Adolescents ages 12 to 17. 20 or 40 mg once daily for up to 8 wk. Children ages 1 to 11. 10 mg once daily for up to 8 wk.
DOSAGE ADJUSTMENT For children weighing 20 kg (44 lb) or more and being treated for healing of erosive esophagitis in GERD, dosage may be increased to 20 mg once daily for 8 wk, if needed. To treat GERD in a patient with a history of erosive esophagitis who can’t take the drug by mouth

IV

, I.V. INJECTION
Adults.20 to 40 mg daily infused for no less than 3 min (I.V. injection) or 10 to 30 min (I.V. infusion). As adjunct to treat duodenal or gastric ulcer associated with Helicobacter pylori DELAYED-RELEASE
Adults.40 mg daily with amoxicillin 1,000 mg b.i.d. and clarithromycin 500 mg b.i.d. for 10 days. To reduce the risk of gastric ulcer formation in patients who are receiving continuous NSAID therapy and who either are over age 60 or have a history of gastric ulcer esomeprazole magnesium 393 E F DELAYED-RELEASE
Adults.20 to 40 mg daily for up to 6 mo. To treat pathological hypersecretory conditions, including Zollinger-Ellison syndrome DELAYED-RELEASE
Adults.40 mg b.i.d.
DOSAGE ADJUSTMENT For patients with severe hepatic insufficiency, maximum 20 mg daily.

Mechanism of Action

Interferes with gastric acid secretion by inhibiting the hydrogen-potassium-adenosine triphosphatase (H1-K1-ATPase) enzyme system, or proton pump, in gastric parietal cells. Normally, the proton pump uses energy from hydrolysis of ATPase to drive H1and chloride (Cl2) out of parietal cells and into the stomach lumen in exchange for potassium (K1), which leaves the stomach lumen and enters parietal cells. After this exchange, H1and Cl2combine in the stomach to form hydrochloric acid (HCl). Esomeprazole irreversibly inhibits the final step in gastric acid production by blocking exchange of intracellular H1and extracellular K1, thus preventing H1from entering the stomach and additional HCl from forming.

Incompatibilities

Don’t give esomeprazole with any other drug through the same I.V. site or tubing.

Contraindications

Hypersensitivity to esomeprazole or its components

Interactions

antimicrobials: Increased esomeprazole level atazanavir, nelfinavir: Decreased blood levels of these diazepam: Possibly increased diazepam level digoxin, iron salts,
ketoconazole: Possibly decreased absorption of these saquinavir: Increased plasma saquinavir level with increased toxicity voriconazole: Increased esomeprazole exposure and risk of adverse effects
warfarin: Possibly increased INR and PT, leading to abnormal bleeding all : Decreased bioavailability of esomeprazole

Side Efect

CNS: Agitation, aggression, depression, dizziness, headache, hallucinations, hepatic encephalopathy
EENT: Blurred vision, dry mouth, mucosal discoloration, sinusitis, stomatitis, taste disturbance
ENDO: Gynecomastia
GI: Abdominal pain; Barrett’s esophagus; benign polyps or nodules; candidiasis; constipation; diarrhea; duodenitis; dyspepsia; esophagitis; esophageal stricture, ulceration, or varices; flatulence; gastric ulcer; gastritis; hepatic failure; hepatitis; jaundice; nausea; pancreatitis
GU: Interstitial nephritis
HEME: Agranulocytosis, pancytopenia
MS: Muscle weakness, myalgia
RESP: Bronchospasm, respiratory tract infection
SKIN: Alopecia, diaphoresis, erythema multiforme, photosensitivity, pruritus, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, infusion site redness or pruritus

Cautions

Give oral esomeprazole at least 1 hour before meals because food decreases bioavailability.
WARNING If patient takes drug with amoxicillin or clarithromycin for H. pylori– related ulcer, severe diarrhea may indicate pseudomembranous colitis. Obtain stool cultures, as ordered.

Always flush I.V. line with normal saline solution injection, lactated Ringer’s injection, or 5% dextrose injection before and after giving esomeprazole intravenously.

For I.V. injection, reconstitute powder with 5 ml of normal saline solution injection and give as a bolus dose over 3 or more minutes. Once reconstituted, drug may be stored at room temperature for up to 12 hours.

For I.V. infusion, reconstitute powder with 5 ml of normal saline solution injection, lactated Ringer’s injection, or 5% dextrose injection. Further dilute reconstituted solution to make a final volume of 50 ml, and infuse over 10 to 30 minutes. Reconstituted drug may be stored at room temperature up to 6 hours if mixed with 5% dextrose injection or up to 12 hours if esomeprazole magnesium 394 mixed with normal saline solution or lactated Ringer’s injection.

Be aware that patient receiving I.V. esomeprazole should be switched to oral form as soon as possible.

PATIENT SAFTY

If patient has trouble swallowing esomeprazole capsules, tell him to open capsule and sprinkle pellets into a tablespoon of cool applesauce. Tell him not to chew pellets and to discard any unused pellets.

Urge patient to tell prescriber if he takes antacids.

Category

Chemical class: Benzodiazepine
Therapeutic class: Sedative-hypnotic

Pregnancy category: X

Controlled substance schedule: IV

Indications

To treat insomnia
Adults. 1 to 2 mg at bedtime.
DOSAGE ADJUSTMENT Starting dose 0.5 mg for small or debilitated elderly patients. Route Onset Peak Duration P.O. Unknown Unknown 6–8 hr

Mechanism of Action

May potentiate effects of gamma-aminobutyric acid (GABA) and other inhibitory neurotransmitters by binding to specific benzodiazepine receptors in limbic and cortical areas of CNS. By binding to these receptors, estazolam increases GABA’s inhibitory effects and blocks cortical and limbic arousal.

Contraindications

Acute angle-closure glaucoma; hypersensitivity to estazolam, other benzodiazepines, or their components; pregnancy; psychosis

Interactions

barbiturates, carbamazepine, phenytoin,
rifampin: Possibly decreased estazolam level carbamazepine: Possibly increased blood carbamazepine level cimetidine, diltiazem, disulfiram, erythromycin, fluoxetine, fluvoxamine, isoniazid, itraconazole, ketoconazole, nefazodone, oral contraceptives, propoxyphene, ranitidine, verapamil: Possibly increased blood level and impaired hepatic metabolism of estazolam clozapine: Possibly cardiac arrest or respiratory depression
CNS depressants: Possibly potentiated CNS depression levodopa: Possibly decreased therapeutic effects of levodopa grapefruit juice: Possibly increased blood level and impaired hepatic metabolism of drug
alcohol use: Possibly potentiated CNS depression

Side Efect

CNS: Amnesia, anxiety, ataxia, confusion, delusions, depression, dizziness, drowsiness, euphoria, headache, hypokinesia, irritability, malaise, nervousness, slurred speech, tremor
CV: Chest pain, palpitations, tachycardia
EENT: Blurred vision, dry mouth, increased salivation, photophobia
GI: Abdominal pain, constipation, diarrhea, nausea, thirst, vomiting
GU: Libido changes
RESP: Respiratory depression
SKIN: Diaphoresis
Other: Physical or psychological dependence

Cautions

Use estazolam with extreme caution in patients with a history of drug or alcohol abuse because of risk of addiction. Expect to give drug for no more than 12 weeks.

Use cautiously in elderly or debilitated patients and those with depression or impaired hepatic, renal, or respiratory function.

Expect to stop drug gradually to prevent withdrawal symptoms. Avoid stopping abruptly if patient has history of seizures.

Monitor respiratory status, especially in patients with respiratory compromise, who are at increased risk for respiratory depression.

If patient takes estazolam for depression, estazolam 395 E F watch for suicidal tendencies, especially when therapy starts or dosage changes.

PATIENT SAFTY

Warn patient not to exceed prescribed time because of risk of addiction.

Because estazolam can reduce alertness, advise patient to avoid hazardous activities until CNS effects of the drug are known.

Advise patient not to drink alcohol or take other CNS depressants during therapy because of the risk of additive effects.

Warn elderly and debilitated patients and those with impaired hepatic or renal function about risk of excessive sedation or mental impairment and need to report them.

If patient takes 2-mg dosage for a long time, warn against stopping drug abruptly.

Category

Chemical class: Estrogen derivative, steroid hormone
Therapeutic class: Antineoplastic, antiosteoporotic agent, ovarian hormone replacement

Pregnancy category: X

Indications

To treat menopausal symptoms (ESTRADIOL) Adult menopausal and postmenopausal women.Starting on day 5 of a cycle, 0.5 to 2 mg daily in cycles of 3 wk on, 1 wk off. Adult postmenopausal women with intact uterus receiving progestin.0.5 to 2 mg daily with daily progestin. Or, 0.5 to 2,mg daily on days 1 through 25 of a 28-day cycle, with progestin starting day 12 or 16 and continuing through day 25 of the cycle; then no on days 26 through 28, as prescribed. VAGINAL RING(ESTRADIOL ACETATE[FEMRING]) Adult women.One ring (0.05 mg or 0.1 mg of estradiol/24 hr) inserted into upper third of vaginal vault and replaced every 3 mo. (ESTRADIOL ACETATE[FEMTRACE]) Adult menopausal and postmenopausal women.Initial: 0.45 mg daily. May be increased to 0.9 mg daily and then 1.8 mg daily as needed. (ETHINYL ESTRADIOL) Adult menopausal and postmenopausal women. 0.02 to 0.05 mg daily in cycles of 3 wk on, 1 wk off. Adult postmenopausal women with intact uterus receiving progestin. 0.02 to 0.05 mg daily with daily progestin; or 0.02 to 0.05 mg daily on days 1 through 25 of a 28day cycle, with progestin starting day 12 or 16 and continuing through day 25; then no on days 26 through 28, as prescribed.
DOSAGE ADJUSTMENT Dosage may be reduced to less than 1 mg daily (estradiol) or 0.05 mg daily (ethinyl estradiol) for patients with only vaginal or vulvar symptoms.

IM

(ESTRADIOL CYPIONATE IN OIL) Adult women.1 to 5 mg as a single dose every 3 to 4 wk as needed.

IM

(ESTRADIOL VALERATE IN OIL) Adult women.10 to 20 mg every 4 wk as needed. TRANSDERMAL(ALORA, ESTRADERM,VIVELLE, VIVELLE-DOT) Adult menopausal and postmenopausal estradiol 396 women.Initial: 0.025 to 0.05 mg daily in cycles of 3 wk on, 1 wk off. One patch applied to trunk or buttocks and replaced twice/wk (every 3 to 4 days). Adjust dosage to control symptoms, as prescribed. TRANSDERMAL (CLIMARA) Adult women.Initial: 0.025 mg daily. One patch applied to trunk or buttocks, replaced every wk. Titrate dosage to control symptoms, as prescribed. Schedule will be cyclic unless patient has had a hysterectomy. TRANSDERMAL (ESCLIM) Adult women.Initial: 0.025 mg daily. One patch applied to upper arm, upper thigh, or buttocks and replaced twice/wk (every 3 to 4 days). Adjust dosage to control symptoms, as prescribed. Use a cyclic schedule, as prescribed, unless patient has had a hysterectomy. TRANSDERMAL(ESTRASORB) Adult women.3.48 g daily in morning. Half of dose (1 pouchful) applied to one thigh and rubbed over entire thigh and calf for 3 min, repeated on other thigh and calf. TRANSDERMAL(ESTROGEL) Adult women. 1.25 g daily applied in thin layer from wrist to shoulder on inside and outside of one arm. TRANSDERMAL(FEMPATCH) Adult women.Initial: 0.025 mg daily. One patch applied to buttocks and replaced every wk. If symptoms aren’t relieved after 4 to 6 wk, increased to two patches every wk, as prescribed. Follow a cyclic schedule, as prescribed, unless patient has had a hysterectomy. TRANSDERMAL MIST(EVAMIST) Adult women.Initial: 1.53 mg (1 spray) once daily in the morning. Dosage may be increased to 3.06 mg (2 sprays) once daily in the morning and then to 4.59 mg (3 sprays) once daily in the morning as needed. To treat menopausal symptoms as combination therapy in patients with an intact uterus TRANSDERMAL ESTRADIOL(ALORA, ESTRADERM, VIVELLE,VIVELLE-DOT), IN COMBINATION WITH ESTRADIOL AND NORETHINDRONE ACETATE (COMBIPATCH) Adult women. 0.05 mg daily estradiol-only transdermal system applied for first 14 days of 28-day cycle and replaced twice/wk, according to product directions. Estradiol and norethindrone acetate transdermal system applied for remaining 14 days of 28day cycle and replaced twice/wk during this period. To treat postmenopausal vaginal and urogenital symptoms VAGINAL CREAM (ESTRACE) Adult women.Initial: 2 to 4 g (200 to 400 mcg) daily for 1 to 2 wk. Then, dosage gradually reduced to half of initial dose, as prescribed, for 1 to 2 wk. Maintenance: 1 g (100 mcg) daily 1 to 3 times/wk for 3 wk, followed by 1 wk of no . Repeat cyclically as needed. VAGINAL RING (ESTRING) Adult women.One ring (7.5 mcg of estradiol/24 hr) inserted into upper third of vaginal vault and replaced every 3 mo. VAGINAL RING(FEMRING) Adult women.One ring (0.05 or 0.1 mg of estradiol/24 hr) inserted into upper third of vaginal vault and replaced every 3 mo. INTRAVAGINAL (VAGIFEM) Adult women.Initial: 10-mcg tablet daily for 2 wk, followed by 1 tablet twice weekly. Dosage increased to 25 mcg, as needed. To prevent osteoporosis secondary to estrogen deficiency due to either natural or surgical menopause (ESTRADIOL) Adult women.At least 0.5 mg daily cyclically or continuously, adjusted as needed to control concurrent menopausal symptoms, as prescribed. (ETHINYL ESTRADIOL) Adult women.At least 0.02 mg daily cyclically or continuously, as prescribed. TRANSDERMAL (ALORA, VIVELLE-DOT) Adult women. Initial: 0.025 mg daily continuously. One patch applied to lower abdomen or buttocks and replaced twice/ wk. Adjust dosage to control symptoms and maintain bone density, as prescribed. TRANSDERMAL (CLIMARA) Adult women. Initial: 0.025 mg daily. One patch applied to trunk or buttocks and replaced every wk. Adjust dosage to control symptoms, as prescribed. Follow a cyclic schedule, as prescribed, unless patient has had a hysterectomy. TRANSDERMAL (ESTRADERM) Adult women. Initial: 0.05 mg daily. One patch applied to trunk or buttocks and replaced twice/wk. Adjust dosage to control estradiol 397 E F symptoms, as prescribed. Follow a cyclic schedule, as prescribed, unless patient has had a hysterectomy. TRANSDERMAL (MENOSTAR) Adult women.Initial: 0.014 mg daily. One patch applied to lower abdomen and replaced every wk. Follow a cyclic schedule, as prescribed, unless patient has had a hysterectomy. To treat estrogen deficiency due to oophorectomy, primary ovarian failure, or female hypogonadism (ESTRADIOL) Adult women.0.5 to 2 mg daily continuously or in cycles of 3 wk on, 1 wk off. (ETHINYL ESTRADIOL) Adult women.For primary ovarian failure or oophorectomy, 0.05 mg t.i.d. initially, then 0.05 mg daily after a few weeks, cyclically or continuously. For female hypogonadism, 0.05 mg once daily to t.i.d. for first 2 wk of a theoretical menstrual cycle. A progestin may be added, as prescribed, during last half of cycle to help induce menses.

IM

(ESTRADIOL CYPIONATE IN OIL) Adult women. 1.5 to 2 mg every mo (for female hypogonadism only).

IM

(ESTRADIOL VALERATE IN OIL) Adult women. 10 to 20 mg every mo as needed. TRANSDERMAL(ALORA, ESTRADERM,VIVELLE) Adult women. Initial: 0.05 mg daily. One patch applied to trunk or buttocks and replaced twice/wk. Titrate dosage to control symptoms, as prescribed. Follow a cyclic schedule, as prescribed, unless patient has had a hysterectomy. TRANSDERMAL (CLIMARA) Adult women. Initial: 0.05 mg daily. One patch applied to trunk or buttocks and replaced every wk. Adjust dosage to control symptoms, as prescribed. Follow a cyclic schedule, as prescribed, unless patient has had a hysterectomy. TRANSDERMAL(ESCLIM) Adult women. Initial: 0.025 mg daily. One patch applied to upper arm, upper thigh, or buttocks and replaced twice/wk (every 3 to 4 days). Adjust dosage to control symptoms, as prescribed. Follow a cyclic schedule, as prescribed, unless patient has had a hysterectomy. TRANSDERMAL (FEMPATCH) Adult women.Initial: 0.025 mg. One patch applied to buttocks and replaced every wk. If symptoms aren’t relieved after 4 to 6 wk, increased to two patches every wk, as prescribed. Follow a cyclic schedule unless patient has had a hysterectomy. To treat dysfunctional uterine bleeding from hormonal imbalance in patients with hypoplastic or atrophic endometrium and without uterine disease TRANSDERMAL(CLIMARA) Adult women.Initial: 0.05 mg daily. One patch applied to trunk or buttocks and replaced every wk. Adjust dosage to control symptoms, as prescribed. Follow a cyclic schedule, as prescribed. TRANSDERMAL (FEMPATCH) Adult women. Initial: 0.025 mg daily. One patch applied to buttocks and replaced every wk. If symptoms aren’t relieved after 4 to 6 wk, increased to two patches every wk, as prescribed. Follow a cyclic schedule, as prescribed. To provide palliative treatment for inoperable, progressive breast cancer in selected men and postmenopausal women (ESTRADIOL)
Adults.10 mg t.i.d. for at least 3 mo. (ETHINYL ESTRADIOL)
Adults. 1 mg t.i.d. for at least 3 mo. To treat advancing, inoperable prostate cancer (ESTRADIOL) Adult men.1 to 2 mg b.i.d. or t.i.d., adjusted or continued, as prescribed, according to patient response. (ETHINYL ESTRADIOL) Adult men. 0.15 to 3 mg daily, adjusted or continued, as prescribed, according to patient response.

IM

(ESTRADIOL VALERATE) Adult men.30 mg every 1 to 2 wk, adjusted or continued, as prescribed, according to patient response.

Mechanism of Action

Increases the rate of DNA and RNA synthesis in cells of female reproductive organs, pituitary gland, hypothalamus, and other target organs. In the hypothalamus, estrogens reduce release of gonadotropin-releasing hormone, which decreases pituitary release of follicle-stimulating hormone and luteinizing hormone. In women, these horestradiol 398 mones are required for normal genitourinary and other essential body functions. At the cellular level, estrogens increase cervical secretions, cause endometrial cell proliferation, and improve uterine tone. Estrogen replacement helps maintain genitourinary function and reduces vasomotor symptoms when estrogen production declines as a result of menopause, surgical removal of ovaries, or other estrogen deficiency states. Estrogen replacement also helps prevent osteoporosis by inhibiting bone resorption. In men, estrogens inhibit pituitary secretion of luteinizing hormone and decrease testicular secretion of testosterone. These actions may decrease prostate tumor growth and lower the level of prostate-specific antigen (PSA).

Contraindications

Active deep vein thrombosis, pulmonary embolism, or history of these conditions; active or recent (within past year) arterial thromboembolic disease, such as stroke or MI; hepatic dysfunction or disease; hypersensitivity to estradiol, ethinyl estradiol, or their components; hypersensitivity to tartrazine dye (contained in 0.02-mg estradiol and ethinyl estradiol tablets); known or suspected breast cancer or history of breast cancer except in appropriately selected patients being treated for metastatic disease; known or suspected estrogen-dependent cancer; pregnancy; undiagnosed abnormal genital bleeding

Interactions

aminocaproic acid: Possibly increased hypercoagulability caused by aminocaproic acid barbiturates, carbamazepine, hydantoins, rifabutin,
rifampin: Possibly reduced activity of estradiol bromocriptine: Possibly decreased therapeutic effects of bromocriptine calcium: Possibly increased calcium absorption corticosteroids: Increased therapeutic and toxic effects of corticosteroids cyclosporine: Increased risk of hepatotoxicity and nephrotoxicity didanosine, lamivudine, zalcitabine: Possibly pancreatitis hepatotoxic , such as isoniazid: Increased risk of hepatitis and hepatotoxicity oral antidiabetic : Decreased therapeutic effects of these somatrem, somatropin: Possibly accelerated epiphyseal maturation tamoxifen: Possibly decreased therapeutic effects of tamoxifen thyroid hormone replacement: Decreased effectiveness vitamin C: Decreased metabolism and possibly increased adverse effects of estradiol
warfarin: Decreased anticoagulant effect grapefruit juice: Decreased estradiol metabolism and possibly increased adverse effects smoking: Increased risk of stroke, pulmonary embolism, thrombophlebitis, and transient ischemic attack

Side Efect

CNS: Dementia, depression, dizziness, headache, migraine headache, stoke
CV: Hypertension, MI, peripheral edema, pulmonary embolism, thromboembolism, thrombophlebitis
EENT: Intolerance of contact lenses, retinal vascular thrombosis, vision changes
ENDO: Breast enlargement, pain, tenderness, or tumors; gynecomastia; hyperglycemia
GI: Abdominal cramps or pain, anorexia, bowel obstruction (vaginal ring), constipation, diarrhea, elevated liver function test results, enlargement of hepatic hemangiomas, gallbladder disease or obstruction, hepatitis, increased appetite, nausea, pancreatitis, vomiting
GU: Amenorrhea, breakthrough bleeding, cervical erosion, clear vaginal discharge, decreased libido (males), dysmenorrhea, endometrial cancer, impotence, increased libido (females), ovarian cancer, pelvic pain, prolonged or heavy menstrual bleeding, ring adherence, testicular atrophy, vaginal candidiasis, worsening of endometriosis
MS: Arthralgia
SKIN: Acne, alopecia, hirsutism, jaundice, melasma, oily skin, purpura, rash, seborrhea, urticaria
Other: Angioedema, folic acid deficiency, hypercalcemia (in metastatic bone disease), toxic shock syndrome (vaginal ring), weight gain estradiol 399 E F

Cautions

WARNING Be aware that estradiol (Estrace) and ethinyl estradiol (Estinyl) are distinct and separate products and that their dosing isn’t equivalent.

Use estradiol cautiously in patients with asthma, chorea, diabetes mellitus, epilepsy, migraine headaches, porphyria, systemic lupus erythematosus, or hepatic hemangiomas because estradiol may worsen these disorders.

Administer oral preparations with or immediately after food to decrease nausea.

For I.M. injection of estradiol cypionate or estradiol valerate, roll vial and syringe between palms to evenly disperse drug. Use at least a 21G needle because of viscosity of oil-based solution. Use a dry, sterile syringe. Inject deep into upper outer quadrant of gluteal muscle. Aspirate before injection to avoid injection into a blood vessel.

Be aware that, in patients who are converting from oral estrogen to transdermal system, oral estrogen should be stopped 1 week before skin patches are applied.

Expect to begin prophylaxis treatment against osteoporosis at the start of menopause.

Be aware that estrogen therapy should be given cyclically or combined with a proges-tin for 10 to 14 days per month in women with an intact uterus to minimize the risk of endometrial hyperplasia.
WARNING Be aware that severe hypercalcemia may occur in patients with bone metastasis due to breast cancer because estrogens influence the metabolism of calcium and phosphorus. Monitor for toxic effects of increased calcium absorption in patients who are predisposed to hypercalcemia or nephrolithiasis.
WARNING Assess patient for possible contact lens intolerance or changes in vision or visual acuity because estrogens can cause keratoconus,leading to increased curvature of the cornea.Be prepared to discontinue drug immediately, as prescribed, if patient experiences sudden partial or complete loss of vision or sudden onset of diplopia, migraine, or proptosis.

Monitor PT test results of patients receiving warfarin for loss of anticoagulant effect because estrogens increase production of clotting factors VII,VIII, IX, and X and promote platelet aggregation.

Watch for elevated liver function test results because estrogens may worsen such conditions as acute intermittent or variegate hepatic porphyria.

Closely monitor patient’s blood pressure. A few patients may experience a substantial increase in blood pressure as an indiosyncratic reaction to estrogen. Monitor patients who already have hypertension for increases in blood pressure because estrogens may cause fluid retention. Also monitor patients with asthma, heart disease, migraines, renal disease, or seizure disorder for exacerbation of these conditions.

Watch for peripheral edema or mild weight gain because estrogens can cause sodium and fluid retention.

Frequently monitor serum glucose level in patients who have diabetes mellitus because estrogens may decrease insulin sensitivity and alter glucose tolerance.
WARNING Expect to stop estrogen therapy in any woman who develops signs or symptoms of cancer; cardiovascular disease, such as stroke, MI, pulmonary embolism, or venous thrombosis; or dementia.

Be aware that exogenous estradiol and progestins may worsen mood disorders, including depression. Monitor patient for anxiety, depression, dizziness, fatigue, insomnia, or mood changes.

Assess skin for melasma (tan or brown patches), which may develop on forehead, cheeks, temples, and upper lip. These patches may persist after drug is stopped.

Check patient’s triglyceride level routinely because, in patients with hypertriglyceridemia, estrogen therapy may increase serum triglyceride level enough to cause pancreatitis and other complications.

Monitor serum PSA level in patients with inoperable prostate cancer to determine if patient is responding to hormone therapy. If patient responds (usually within 3 months), expect therapy to continue until disease is significantly advanced.

Monitor thyroid function test results in patients with hypothyroidism because long-term use of ethinyl estradiol may decrease effectiveness of thyroid therapy. estradiol 400

Expect to stop estrogen therapy several weeks before patient undergoes major surgery, as prescribed, because certain procedures are associated with prolonged immobilization and therefore pose a risk of thromboembolism.

If patient takes thyroid hormone replacement therapy, monitor her for increased signs and symptoms of hypothyroidism because estradiol may increase thyroid binding globulin levels, which may make the patient’s current dose of thyroid hormone insufficient.

PATIENT SAFTY

Before therapy starts, inform patient of risks involved in estrogen therapy, such as increased risk of breast, endometrial, or ovarian cancer; cardiovascular disease; dementia (if age 65 or over); gallbladder disease; and vision abnormalities.

Advise patient to remain recumbent for at least 30 minutes after applying estradiol vaginal cream. Inform her that she may use a sanitary napkin (but not a tampon) to protect clothing after application.

Teach patient proper application and use of transdermal patch. Instruct her not to apply patch to breasts, waistline, or other areas where it may not adhere properly. Advise her to rotate application sites at least weekly and to remove old patch before applying new one. If patch falls off, instruct her to reapply it to another area or to apply a new patch and continue the original treatment schedule. Caution her not to expose patch to sun for long periods. Explain that she may bathe while wearing the patch.

Teach patient to apply Estrogel to clean, dry skin of one arm, using applicator. Stress importance of transferring all of the gel from applicator to arm. Tell patient to spread gel as thinly as possible over entire inside and outside of arm from wrist to shoulder. Advise her to wash her hands with soap and water afterward and to avoid fire and smoking until gel has dried because it’s flammable. Tell patient never to apply gel to breasts. Warn that gel is alcohol-based and that patient should avoid fire, flame, or smoking until gel has dried.

Inform patient that each pouch of Estrasorb contains half of daily dose. Instruct her to apply emulsion to clean, dry skin on top of thigh and to rub it into entire thigh and calf for 3 minutes. Tell her to rub any excess emulsion onto her buttocks. Then, advise her to repeat procedure on her other thigh and calf using the second pouch. Tell her to wash her hands with soap and water after the application and to dress only after affected areas are dry.

Teach patient proper use of estradiol vaginal ring. Instruct her to insert ring in upper third of vagina, to keep it there for 90 days, and then to remove it and insert a new ring. Or she may remove it during the 90-day dosage period, rinse it with lukewarm (not hot or boiling) water, and reinsert it as needed for personal hygiene. Remind patient that she shouldn’t be able to feel the ring when it’s in place. If she does, she should use a finger to push the ring farther into her vagina. If vaginal wall ulcertation or erosion occurs, suggest that patient leave ring out and not replace it until healing is complete to keep ring from adhering to healing tissue.

Instruct patient using estradiol vaginal ring to remove ring immediately and contact prescriber if she develops fever, nausea, vomiting, diarrhea, muscle pain, dizziness, faintness, or a sunburn rash on face or body that may suggest a rare but serious bacterial infection called toxic shock syndrome. Also ugre patient to seek prompt medical care if ring becomes attached to vaginal wall (rare), making removal difficult.

Instruct patient prescribed transdermal Evamist to prime the pump of a new device before the first dose by holding the container upright with the cover in place and spraying 3 sprays. Then, to deliver a dose, she should spray the mist on the inner aspect of her forearm starting near the elbow. Instruct her to let the mist dry for 2 minutes and to not wash the area for at least 30 minutes.

Inform patient receiving estradiol treatment that she should have an annual pelvic examination to screen for cervical dysplasia.

Tell patient who has an intact uterus and is prescribed transdermal Menostar that she will need to receive progestin for 14 estradiol 401 E F days every 6 to 12 months and have an endometrial biopsy yearly.

Category

Chemical class: Estrogen derivative, steroid hormone
Therapeutic class: Antiosteoporotic agent, ovarian hormone replacement

Pregnancy category: X

Indications

To treat moderate to severe vasomotor menopausal symptoms (CENESTIN, PREMARIN)
Adults.0.3 to 1.25 mg daily (Cenestin, Premarin) or cyclically 25 days on, 5 days off (Premarin only). Dosage increased as needed to control symptoms. (ENJUVIA)
Adults. 0.625 mg daily. Dosage increased as needed to control symptoms. (PREMPRO)
Adults.0.3 mg conjugated estrogens and 1.5 mg medroxyprogesterone daily. Increased up to 0.625 mg conjugated estrogens and 5 mg medroxyprogesterone daily as needed. (PREMPHASE)
Adults.0.625 mg conjugated estrogens daily on days 1 through 14 and combination product (0.625 mg conjugated estrogens and 5 mg medroxyprogesterone) on days 15 through 28. To treat vaginal and vulvar atrophy (CENESTIN, PREMARIN)
Adults. 0.3 to 1.25 mg daily (Cenestin, Premarin) or cyclically 25 days on, 5 days off (Premarin only). Dosage increased as needed to control symptoms. (PREMPRO)
Adults.0.3 mg conjugated estrogens and 1.5 mg medroxyprogesterone daily. Increased up to 0.625 mg conjugated estrogens and 5 mg medroxyprogesterone daily as needed. (PREMPHASE)
Adults.0.625 mg conjugated estrogens daily on days 1 through 14 and combination product (0.625 mg conjugated estrogens and 5 mg medroxyprogesterone) on days 15 through 28. To treat atrophic vaginitis and vaginal and vulvar atrophy VAGINAL CREAM (PREMARIN)
Adults.0.5 to 2 g daily in cycles of 3 wk on, 1 wk off. To treat moderate to severe vaginal dryness and pain with intercourse and symptoms of vulvar and vaginal atrophy in menopause (ENJUVIA)
Adults.0.3 mg daily. VAGINAL CREAM(PREMARIN)
Adults. 0.5 g twice/wk. Or, 0.5 g daily for 21 days followed by 7 days off, with cycle repeated every 28 days. VAGINAL CREAM(SCE-A)
Adults. 1 g daily for 1 wk, followed by 1 g twice/wk. To prevent postmenopausal osteoporosis (CENESTIN, PREMARIN)
Adults. 0.625 mg daily continuously or in cycles of 25 days on, 5 days off. (PREMPRO)
Adults. 0.3 mg conjugated estrogens and 1.5 mg medroxyprogesterone daily. Increased to 0.625 mg conjugated estrogens and 5 mg medroxyprogesterone daily as needed. (PREMPHASE)
Adults.0.625 mg conjugated estrogens daily estrogens (conjugated) 402 on days 1 through 14 and combination product (0.625 mg conjugated estrogens and 5 mg medroxyprogesterone) on days 15 through 28. To provide palliative treatment for advanced androgen-dependent prostate cancer (PREMARIN)
Adults. 1.25 to 2.5 mg t.i.d. To provide palliative treatment for metastatic breast cancer (PREMARIN)
Adults.10 mg t.i.d. for 3 mo or longer. To treat dysfunctional uterine bleeding

IV

,

IM

(PREMARIN)
Adults.25 mg, repeated in 6 to 12 hr if needed. To treat estrogen deficiency from oophorectomy or primary ovarian failure (PREMARIN)
Adults.1.25 mg daily in cycles of 3 wk on, 1 wk off. To treat female hypogonadism (PREMARIN)
Adults. 0.3 to 0.625 mg daily in cycles of 3 wk on, 1 wk off. Increased as needed every 6 to 12 mo.

Mechanism of Action

Increase the rate of DNA and RNA synthesis in the cells of female reproductive organs, hypothalamus, pituitary glands, and other target organs. In the hypothalamus, estrogens reduce the release of gonadotropin-releasing hormone, which decreases pituitary release of follicle-stimulating hormone and luteinizing hormone. In women, these hormones are required for normal genitourinary and other essential body functions. At the cellular level, estrogens increase cervical secretions, cause endometrial cell proliferation, and increase uterine tone. Estrogen replacement helps maintain genitourinary function and reduce vasomotor symptoms when estrogen production declines from menopause, surgical removal of ovaries, or other estrogen deficiency. Estrogen also helps prevent osteoporosis by keeping bone resorption from exceeding bone formation. In men, estrogens inhibit pituitary secretion of luteinizing hormone and decrease testicular secretion of testosterone. These actions may decrease prostate tumor growth and lower the level of prostate-specific antigen.

Contraindications

Active deep vein thrombosis, pulmonary embolism, or history of these conditions; active or recent (within past year) arterial thromboembolic disease such as stroke or MI; hepatic dysfunction or disease; hypersensitivity to estrogens or their components; known or suspected breast cancer or history of breast cancer; known or suspected estrogen-dependent cancer; pregnancy; undiagnosed abnormal genital bleeding

Incompatibilities

Don’t combine I.V. estrogens with acid solutions, ascorbic acid, and protein hydrolysate because they’re incompatible.

Interactions

aminocaproic acid: Possibly increased level of hypercoagulability caused by aminocaproic acid barbiturates, carbamazepine, hydantoins, rifabutin,
rifampin: Possibly reduced activity of estrogen and medroxyprogesterone bromocriptine: Possibly interference with bromocriptine’s therapeutic effects calcium: Possibly increased calcium absorption corticosteroids: Increased therapeutic and toxic effects of corticosteroids cyclosporine: Increased risk of hepatotoxicity and nephrotoxicity didanosine, lamivudine, zalcitabine: Possibly pancreatitis hepatotoxic (such as isoniazid): Increased risk of hepatitis and hepatotoxicity oral antidiabetic : Decreased therapeutic effects of these somatrem, somatropin: Possibly accelerated epiphyseal maturation tamoxifen: Possibly interference with tamoxifen’s therapeutic effects thyroid hormone replacement: Decreased effectiveness
warfarin: Decreased anticoagulant effect smoking: Increased risk of stroke, pulmonary embolism, thrombophlebitis, and transient ischemic attack

Side Efect

CNS: Asthenia, dementia, depression, dizziness, growth benign meningioma, estrogens (conjugated) 403 E F headache, insomnia, migraine headache, mood disturbance, nervousness, paresthesia, stroke
CV: Hypertension, MI, peripheral edema, thromboembolism, thrombophlebitis, vasodilation
EENT: Intolerance of contact lenses, pharyngitis, retinal vascular thrombosis, rhinitis, sinusitis
ENDO: Breast enlargement, pain, tenderness, or tumors; gynecomastia (men); hot flashes; hyperglycemia
GI: Abdominal cramps or pain, anorexia, cholestatic jaundice, constipation, diarrhea, flatulence, gallbladder disease or obstruction, hepatic hemangioma enlargement, hepatitis, increased appetite, ischemic colitis, nausea, pancreatitis, vomiting
GU: Amenorrhea, breakthrough bleeding, cervical erosion, clear vaginal discharge, decreased libido (men), dysmenorrhea, endometrial cancer or hyperplasia, impotence, increased libido (women), leukorrhea, ovarian cancer, prolonged or heavy menstrual bleeding, testicular atrophy, uterine leiomyomata enlargement, vaginal candidiasis, vaginitis, vaginal site reactions (vaginal administration only) such as burning, irritation, and genital pruritus
MS: Arthralgias, back pain
RESP: Bronchitis, increased cough, pulmonary embolism
SKIN: Acne, alopecia, chloasma, erythema multiforme, erythema nodosum, hemorrhagic eruption, hirsutism, melasma, oily skin, pruritus, purpura, rash, seborrhea, urticaria
Other: Anaphylaxis, angioedema, flu syndrome, folic acid deficiency, hypercalcemia (in metastatic bone disease), weight gain

Cautions

Use conjugated estrogens cautiously in patients with severe hypocalcemia because a sudden increase in serum calcium level may cause

Side Efect

.

Reconstitute conjugated estrogens with normal saline solution, dextrose, or invert sugar solution and use within a few hours. Discard solution that contains precipitate.
WARNING Monitor serum calcium level to detect severe hypercalcemia in patients with bone metastasis from breast cancer.

Watch for elevated liver function test results because estrogen and progestins may worsen such conditions as acute intermittent or variegate hepatic porphyria.

Assess hypertensive patients for increases in blood pressure because estrogens may cause fluid retention.

Monitor patients with asthma, diabetes mellitus, endometriosis, heart disease, lupus erythematosus, migraine headaches, renal disease, or seizure disorder for worsening of these conditions.

If patient takes warfarin, assess PT for loss of anticoagulant effects because estrogens increase production of clotting factors and promote platelet aggregation.

Expect to stop drug during periods of immobilization, 4 weeks before elective surgery, and if jaundice develops.
WARNING Expect to stop estrogen combination therapy in any woman who develops signs or symptoms of cancer; cardiovascular disease, such as MI, pulmonary embolism, venous thrombosis, or stroke; or dementia.

Check triglyceride level routinely because, in hypertriglyceridemia, estrogen therapy may increase triglycerides enough to cause pancreatitis and other complications.

If patient takes thyroid hormone replacement therapy, monitor her for increased signs and symptoms of hypothyroidism because estrogen may increase thyroid binding globulin level, which may make the patient’s current dose of thyroid hormone insufficient.

Estrogen may worsen mood disorders, including depression. Monitor patient for depression, fatigue, insomnia, or mood changes.

PATIENT SAFTY

Explain the risks of estrogen therapy, including increased risk of breast, endometrial, or ovarian cancer; cardiovascular disease; dementia; and gallbladder disease.

Instruct patient how to use vaginal cream and to cleanse plunger by removing it from barrel and washing it with mild soap and warm water after each use.

Urge patient to immediately report breakthrough bleeding to prescriber.

Instruct patient to perform monthly breast self-examination and to comply with all prescribed follow-up examinations.

Warn female patient that long-term use estrogens (conjugated) 404 may increase risk of dementia, heart disease, stroke, gallbladder disease, and breast or endometrial cancer.

Inform patient that estrogen vaginal cream may alter effectiveness of condoms, diaphragms, or cervical caps made of latex or rubber.

Category

Chemical class: Pyrrolopyrazine derivative of cyclopyrrolone class
Therapeutic class: Sedative-hypnotic

Pregnancy category: C

Controlled substance schedule: IV

Indications

To treat insomnia
Adults.Initial: 2 mg immediately at bedtime. May be increased to 3 mg at bedtime, as needed. Maintenance: 3 mg at bedtime.
DOSAGE ADJUSTMENT For elderly patients who have trouble falling asleep or patients with severe hepatic impairment, dosage decreased to 1 mg at bedtime. For elderly patients who have trouble staying asleep, dosage may be increased to 2 mg at bedtime. Route Onset Peak Duration P.O. Unknown 1 hr Unknown

Mechanism of Action

May potentiate effects of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) by binding close to or with benzodiazepine receptors in limbic and cortical areas of the CNS. By binding to these receptor sites and areas, eszopiclone increases GABA’s inhibitory effects and blocks cortical and limbic arousal, thereby inducing and maintaining sleep.

Contraindications

Hypersensitivity to eszopiclone or its components

Interactions

clarithromycin, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, troleandomycin: Increased eszopiclone level
rifampin: Decreased eszopiclone level
alcohol use: Additive effect on psychomotor performance

Side Efect

CNS: Agitation, anxiety, bizarre behavior such as sleep driving, confusion, depersonalization, depression, dizziness, hallucinations, headache (including migraine), nervousness, neuralgia, somnolence, unusual dreams
CV: Chest pain, peripheral edema
EENT: Dry mouth, taste perversion
ENDO: Gynecomastia
GI: Diarrhea, hepatitis, indigestion, nausea, vomiting
GU: Decreased libido, dysmenorrhea, UTI
RESP: Asthma, respiratory tract infection
SKIN: Pruritus, rash
Other: Generalized pain, heat stroke, viral infection

Cautions

Use eszopiclone cautiously in patients with severe mental depression or reduced respiratory function; drug may intensify mental depression and lead to respiratory depression.

PATIENT SAFTY

Instruct patient not to exceed prescribed eszopiclone dosage and not to stop drug abruptly because withdrawal symptoms may occur.

Because eszopiclone can reduce alertness, advise patient to take drug immediately before bedtime and to avoid potentially hazardous activities until drug’s CNS effects are known.

Urge patient to avoid alcohol and CNS depressants because of additive effects.

Advise woman of childbearing age to notify prescriber if she becomes or intends to become pregnant during therapy.

Explain that sleep may be disturbed for the first few nights after therapy.

Warn patient and caregiver that some patients have performed bizarre activities after taking drug, such as driving the car, preparing and eating food, making phone calls, or having sex while not fully awake and often with no memory of the event. These episodes usually occur in patients eszopiclone 405 E F who have taken the drug with alcohol or other CNS depressant or who have exceeded the recommended dose. If such an episode occurs, the prescriber should be notified and eszopiclone therapy discontinued immediately.

Category

Chemical class: Dimeric recombinant human p75 tumor necrosis factor receptor
Therapeutic class: Disease-modifying antirheumatoid drug

Pregnancy category: B

Indications

To reduce signs and symptoms of rheumatoid or psoriatic arthritis, slow structural damage in active arthritis, and improve physical function in patients with psoriatic arthritis, alone or in combination with methotrexate SUBCUTANEOUS INJECTION
Adults. 50 mg once/wk on same day each wk. To reduce signs and symptoms of active ankylosing spondylitis SUBCUTANEOUS INJECTION
Adults. 50 mg once/wk on same day each wk. To reduce signs and symptoms of juvenile rheumatoid arthritis SUBCUTANEOUS INJECTION Children ages 4 to 17. 0.4 mg/kg twice/wk 3 to 4 days apart for 3 to 7 mo. Or, 0.8 mg/ kg once/wk on same day each wk for 3 to 7 mo. Maximum: 25 mg twice/wk or 50 mg weekly. To treat chronic moderate-to-severe plaque psoriasis in candidates for systemic therapy or phototherapy SUBCUTANEOUS INJECTION
Adults. Initial: 50 mg twice/wk 3 to 4 days apart for 3 mo; then reduced to 50 mg/wk. To reduce signs and symptoms of moderately to severely active polyarticular juvenile idiopathic arthritis SUBCUTANEOUS INJECTION Children ages 2 to17. 0.8 mg/kg/wk. Maximum: 50 mg/wk.

Incompatibilities

Don’t combine etanercept with other .

Contraindications

Hypersensitivity to etanercept, hamster protein, or their components; sepsis or risk of it

Interactions

cyclophosphamide: Possibly increased risk of malignancy sulfasalazine: Possibly decreased neutrophil count

Side Efect

CNS: Asthenia, chills, dizziness, fever, headache, multiple sclerosis, seizures
CV: Congestive heart failure, hypertension, hypotension, peripheral edema
EENT: Optic neuritis, pharyngitis, rhinitis, sinusitis
GI: Abdominal abscess, abdominal pain, autoimmune hepatitis, cholecystitis, diarrhea, gastroenteritis, indigestion, nausea, noninfectious hepatitis, vomiting
GU: Pyelonephritis
HEME: Aplastic anemia, neutropenia, pancytopenia
MS: Osteomyelitis, septic arthritis, transverse myelitis
RESP: Bronchitis, cough, pneumonia, upper respiratory tract infection
SKIN: Cellulitis, foot abscess, leg ulceration, pruritus, rash, urticaria
Other: Angioedema; injection site edema, erythema, itching, and pain; malignancy, such as leukemia or lymphoma; sepsis; varicella infection

Cautions

Screen patient for latent tuberculosis with a tuberculin skin test before starting etanercept therapy. If test is positive, expect to give treatment, as ordered, before starting etanercept. Also screen patient for hepatitis B. If present, expect etanercept therapy to be withdrawn because antirheumatic therapies like etanercept may reactivate hepatitis B.

Use cautiously in patients with a history of recurrent infection, underlying conditions that may predispose them to infections, or an existing chronic, latent, or localized infection because etanercept increases their risk of infection.

Use cautiously in patients with COPD, and etanercept 406 monitor respiratory status closely because etanercept therapy may increase patient’s risk of adverse respiratory reactions.

Use cautiously in patients with preexisting or recent onset CNS demyelinating disorders because drug may worsen these conditions. Also use cautiously in patients with heart failure because drug may worsen it.

Tumor necrosis factor antagonists shouldn’t be given with etanercept because doing so increases the risk of serious infection.
WARNING Don’t use the diluent provided with etanercept (bacteriostatic water for injection, USP, with 0.9% benzyl alcohol) for patients who have benzyl alcohol hypersensitivity. Instead, use sterile water for injection for these patients.
WARNING If you have a latex allergy, don’t handle needle cover of diluent syringe because it contains dry natural rubber.

When giving etanercept to children, don’t use the 25-mg prefilled syringe if the child weighs less than 31 kg (68 lb). The 50-mg prefilled syringe or SureClick autoinjector may be used for children who weigh 63 kg (138 lb) or more.
WARNING Expect to stop etanercept if patient develops sepsis.

Avoid giving live-virus vaccines to patients who are taking etanercept because drug decreases immune response and increases risk of secondary transmission of vaccine virus.

Monitor immunosuppressed patients for evidence of acute or chronic infection, including chills, fever, and tachycardia, because etanercept decreases defenses against infection. It also increases the risk of developing malignant tumors.

Continue giving corticosteroids, NSAIDs, and other analgesics, as prescribed, during etanercept therapy.

Malignancies, especially lymphomas and leukemias, have been reported rarely in patients taking tumor necrosis factor etanercept 407 E F TNF receptor Cell membrane Macrophage Etanercept bound to TNF TNF Inflammation TNF receptor Cell membrane Macrophage Etanercept bound to TNF TNF Inflammation

Mechanism of Action

Etanercept reduces joint inflammation from rheumatoid arthritis by binding with tumor necrosis factor (TNF), a cytokine, or protein, that plays an important role in normal inflammatory and immune responses. In rheumatoid arthritis, the immune and inflammatory process triggers release of TNF, mainly from macrophages. TNF then binds to TNF receptors on cell membranes, as shown below left. This action renders TNF biologically active and triggers a cascade of inflammatory events that results in increased inflammation of the synovial membrane, release of destructive lysosomal enzymes, and further joint destruction. Etanercept binds to TNF and prevents it from binding with TNF receptors on the cell membranes, as shown below right. This action renders bound TNF biologically inactive, prevents TNF-mediated cellular responses, and significantly reduces inflammatory activity. blockers such as etanercept. Children, adolescents, and patients with rheumatoid arthritis, especially those with very active disease, are at greatest risk. Monitor closely.

PATIENT SAFTY

Inform patient that etanercept is given by a small injection under the skin, and teach him proper injection technique if needed.

If patient will take 50-mg dose, explain that a prefilled syringe is available to eliminate the need to mix or draw up drug.

If patient will take less than 50-mg dose or prefers not to use prefilled syringe, advise him to use drug as soon as possible after dissolving powder. Dissolved powder may be kept in refrigerator for up to 6 hours after mixing and then should be discarded.

Instruct patient to rotate injection sites among thigh, stomach, and upper arms and to avoid areas that are tender, red, bruised, or hard. Advise him to keep each site at least 10 away from a previous site.

Urge patient to use needles and syringes once and discard in puncture-proof container.

Caution patient that the risk of malignancies such as leukemia and lymphoma may be higher in those who take etanercept, especially children and adolescents. Tell him to seek medical attention promptly for any suspicious signs and symptoms.

Urge patient to consult prescriber immediately if he develops an infection because drug may decrease the body’s infectionfighting ability.

Caution patient who hasn’t had chickenpox to contact prescriber right away if he’s exposed because he may develop a more serious infection.

Urge patient to seek immediate emergency care if he develops a persistent fever, bruising, bleeding, or pallor while taking drug.

Category

Chemical class: Ketone derivative of anyloxyacetic acid
Therapeutic class: Diuretic

Pregnancy category: B

Indications

To promote diuresis in heart failure; hepatic cirrhosis; renal disease; ascites of short duration caused by cancer, idiopathic edema, or lymphedema; and edema in children (excluding infants with congenital heart disease or nephrotic syndrome)

ORALL

,
Adults. Initial: 50 to 100 mg daily as a single dose or in divided doses. Dosage increased by 25 to 50 mg daily, if needed. Maintenance: 50 to 200 mg daily. Maximum: 400 mg daily. Children (except infants). Initial: 25 mg daily. Dosage increased in 25-mg increments daily, if needed.
IV:
Adults. Initial: 50 mg or 0.5 to 1 mg/kg. Dose repeated in 2 to 4 hr, if needed, then every 4 to 6 hr based on patient response. In an emergency, dose repeated every 1 hr, if needed. Maximum: 100 mg as single dose. Route Onset Peak Duration P.O. 30 min 2 hr 6–8 hr I.V. 5 min 15–30 min 2 hr

Mechanism of Action

Probably inhibits the sulfhydryl-catalyzed enzyme systems that cause sodium and chloride resorption in the proximal and distal tubules and the ascending limb of the loop of Henle. These inhibitory effects increase urinary excretion of sodium, chloride, and water, causing profound diuresis. Drug also increases the excretion of potassium, hydrogen, calcium, magnesium, bicarbonate, ammonium, and phosphate.

Contraindications

Anuria; hypersensitivity to ethacrynic acid, ethacrynate sodium, sulfonylureas, or their components; infancy; severe diarrhea

Interactions

ACE inhibitors, antihypertensives: Possibly hypotension aminoglycosides: Increased risk of ototoxicity amiodarone: Increased risk of arrhythmias ethacrynic acid 408 amphotericin B: Increased risk of electrolyte imbalances, nephrotoxicity, and ototoxicity anticoagulants, thrombolytics: Possibly potentiated anticoagulation and risk of hemorrhage corticosteroids: Increased risk of gastric hemorrhage digoxin: Increased risk of digitalis toxicity insulin, oral antidiabetic : Possibly increased serum glucose level and decreased therapeutic effects of these lithium: Increased risk of lithium toxicity neuromuscular blockers: Possibly increased neuromuscular blockade
NSAIDs: Possibly decreased effects of ethacrynic acid sympathomimetics: Possibly interference with hypotensive effects of ethacrynic acid and ethacrynate sodium
alcohol use: Possibly potentiated hypotensive and diuretic effects of ethacrynic acid and ethacrynate sodium

Side Efect

CNS: Confusion, fatigue, headache, malaise, nervousness
CV: Orthostatic hypotension
EENT: Blurred vision, hearing loss, ototoxicity (ringing or buzzing in ears), sensation of fullness in ears, yellow vision
ENDO: Hyperglycemia, hypoglycemia
GI: Abdominal pain, anorexia, diarrhea, dysphagia, GI bleeding (I.V. form), nausea, vomiting
GU: Hematuria (I.V. form), interstitial nephritis, polyuria
HEME: Agranulocytosis, severe neutropenia, thrombocytopenia
SKIN: Rash
Other: Hyperuricemia, hypochloremic alkalosis, hypokalemia, hypomagnesemia, hyponatremia, hypovolemia, infusion site irritation and pain

Cautions

WARNING Give ethacrynic acid and ethacrynate sodium cautiously in patients with advanced hepatic cirrhosis, especially those with a history of electrolyte imbalance or hepatic encephalopathy; both forms of drug may lead to lethal hepatic coma.

Dilute ethacrynate sodium with D5W or normal saline solution for I.V. infusion. Discard unused portion after 24 hours.

Don’t use diluted ethacrynate sodium that’s cloudy or opalescent.

Infuse I.V. ethacrynate sodium slowly over 30 minutes.

Weigh patient daily, and assess him for signs and symptoms of electrolyte imbalances and dehydration.

Monitor blood pressure and fluid intake and output, and check laboratory test results.

Report significant changes. Prescriber may reduce dosage or temporarily stop drug.

If hypokalemia develops, administer replacement potassium, as ordered.

Monitor serum glucose level frequently, especially if patient has diabetes mellitus; both forms of drug may cause hyperglycemia or hypoglycemia.

Notify prescriber if patient experiences hearing loss, vertigo, or ringing, buzzing, or sense of fullness in his ears. Drug may need to be discontinued.

PATIENT SAFTY

Instruct patient to take the last dose of ethacrynic acid several hours before bedtime to avoid sleep interruption from diuresis. If patient receives once-daily dosing, advise him to take the dose in the morning to avoid sleep disturbance caused by nocturia.

Suggest that patient take ethacrynic acid with food or milk to reduce the likelihood of GI distress.

Advise patient to change position slowly to minimize effects of orthostatic hypotension, especially if he also takes an antihypertensive.

Unless contraindicated, urge patient to eat more high-potassium and to take a potassium supplement, if prescribed, to prevent hypokalemia.

Caution patient not to drink alcohol, stand for prolonged periods, or exercise during hot weather because these activities may exacerbate orthostatic hypotension.

Instruct patient to notify prescriber if he has diarrhea; buzzing, fullness, or ringing in his ears; hearing loss; severe nausea; vertigo; or vomiting. Drug may need to be discontinued.

Remind diabetic patients to check their serum glucose levels often for changes.

Category

Chemical class: Diisopropylethylene diamide derivative
Therapeutic class: Antitubercular

Pregnancy category: C

Indications

As adjunct to treat tuberculosis and atypical mycobacterial infections caused by Mycobacterium tuberculosis Adults and adolescents who haven’t received previous antituberculotic therapy.15 mg/kg daily. Adults and adolescents who have received antituberculotic therapy. 25 mg/kg daily; after 60 days, decreased to 15 mg/kg daily.

Mechanism of Action

May suppress bacterial multiplication by interfering with RNA synthesis in susceptible bacteria that are actively dividing.

Contraindications

Hypersensitivity to ethambutol or its components, inability to report changes in vision, optic neuritis

Interactions

antacids that contain aluminum hydroxide: Decreased absorption of ethambutol other neurotoxic : Increased risk of neurotoxicity, such as optic and peripheral neuritis

Side Efect

CNS: Burning sensation or weakness in arms and legs, confusion, disorientation, dizziness, fever, headache, malaise, paresthesia, peripheral neuritis
EENT: Blurred vision, decreased visual acuity, eye pain, optic neuritis, red-green color blindness
GI: Abdominal pain, anorexia, hepatic dysfunction, nausea, vomiting
HEME: Leukopenia, neutropenia, thrombocytopenia
MS: Arthralgia, gouty arthritis, joint pain
RESP: Pulmonary infiltrates
SKIN: Dermatitis, erythema multiforme, pruritus, rash
Other: Anaphylaxis, hypersensitivity syndrome (rash or exfoliative dermatitis, eosinophilia, and one of the following: hepatitis, pneumonitis, nephritis, myocarditis, pericarditis), lymphadenopathy

Cautions

Expect prescriber to refer patient for an ophthalmologic examination that includes tests for visual fields, acuity, and red-green color blindness before taking ethambutol and monthly thereafter. This is especially likely if therapy is prolonged or dosage exceeds 15 mg/kg daily.
WARNING Notify prescriber immediately if patient develops vision changes, and expect ethambutol to be stopped if they occur.

Expect to give the patient at least one other antituberculotic with ethambutol, as prescribed, because bacteria may become resistant quickly to a single drug.

Monitor laboratory test results for changes in liver function or for increased serum uric acid level if patient has gouty arthritis or impaired renal function. Notify prescriber of any abnormalities.

Obtain a monthly sputum specimen, as ordered, to check bacteriologic response in sputum-positive patient.

Knowthat successful ethambutol therapy typically takes 6 to 12 months but may take years.

PATIENT SAFTY

Teach patient to recognize possible adverse reactions to ethambutol.

Advise patient to take drug with food if he experiences adverse GI reactions.

Instruct patient to take a missed dose as soon as he remembers, unless it’s nearly time for the next dose, but not to doubledose.

Explain that ethambutol therapy may last months or years and that compliance is essential.

Advise patient to notify prescriber if no improvement occurs within 3 weeks of starting ethambutol therapy; if bothersome or severe

Side Efect

occur; if his vision changes; or if a rash, fever, or joint pain (possible hypersensitivity) develops.

Category

Chemical class: Chlorinated tertiary acetylenic carbinol
Therapeutic class: Sedative-hypnotic

Pregnancy category: C

Controlled substance schedule: IV

Indications

To provide short-term relief from insomnia
Adults.0.5 to 1 g at bedtime for no longer than 1 wk. Route Onset Peak Duration P.O. 15–60 min Unknown 5 hr

Mechanism of Action

Exerts sedative-hypnotic, muscle relaxant, and anticonvulsant effects possibly by depressing the reticular activating system.

Contraindications

Hypersensitivity to ethchlorvynol or its components, porphyria

Interactions

CNS depressants, tricyclic antidepressants: Increased CNS depression oral anticoagulants: Decreased anticoagulant effects
alcohol use: Increased CNS depression

Side Efect

CNS: Ataxia, dizziness, facial numbness, fatigue, light-headedness, syncope, unsteadiness, weakness
CV: Hypotension
EENT: Blurred vision, unpleasant aftertaste
GI: Epigastric pain, indigestion, nausea, vomiting
HEME: Thrombocytopenia
SKIN: Jaundice, rash, urticaria
Other: Physical and psychological dependence

Cautions

If patient awakens too early after taking 0.5 or 0.75 g of ethchlorvynol at bedtime, ask prescriber if he may take a single supplemental dose of 200 mg.

Assess for signs of addiction if patient has taken drug for 2 weeks or longer.

Be aware that ethchlorvynol shouldn’t be given for longer than 1 week. If patient has received prolonged therapy, expect to discontinue drug gradually to prevent withdrawal symptoms. Notify prescriber if you detect evidence of withdrawal, such as diaphoresis, hallucinations, irritability, muscle twitching, nausea, nervousness, restlessness, seizures, sleep disturbance, tremor, vomiting, and weakness.

PATIENT SAFTY

Caution patient not to exceed prescribed dosage or dosing frequency because of ethchlorvynol’s habit-forming potential. Instruct him not to use drug for more than 1 week.

Advise patient to take ethchlorvynol with food or milk to minimize adverse GI reactions.

If patient has taken long-term ethchlorvynol therapy, warn against stopping drug abruptly; advise him to contact prescriber for guidelines to reduce dosage.

Direct patient to avoid alcohol and other CNS depressants during ethchlorvynol therapy because they increase the risk of

Side Efect

.

Advise patient to avoid potentially hazardous activities until drug’s CNS effects are known.

Category

Chemical class: Thiamide analogue of isonicotinic acid
Therapeutic class: Antituberculotic

Pregnancy category: Not rated

Indications

As adjunct to treat tuberculosis
Adults. 0.5 to 1 g daily in divided doses every 8 to 12 hr, together with other antituberculotics. Maximum: 1 g daily. Children.15 to 20 mg/kg daily in divided doses every 8 to 12 hr, together with other antituberculotics. Maximum: 750 mg daily. ethchorvynol;ethionamide 411 E F

Mechanism of Action

May inhibit peptide synthesis, resulting in bacteriostatic action against Mycobacterium tuberculosis.

Contraindications

Hypersensitivity to ethionamide or its components, severe hepatic damage

Interactions

cycloserine: Increased risk of adverse CNS effects, especially seizures other neurotoxic : Increased risk of neurotoxicity, such as optic and peripheral neuritis

Side Efect

CNS: Burning or pain in arms and legs, clumsiness, confusion, depression, mental or mood changes, paresthesia, unsteadiness
CV: Orthostatic hypotension
EENT: Blurred vision, eye pain, increased salivation, metallic taste, optic neuritis, stomatitis, vision loss
ENDO: Goiter, hypoglycemia, hypothyroidism
GI: Anorexia, hepatitis, nausea, vomiting
SKIN: Jaundice, rash

Cautions

Use ethionamide cautiously in patients with a history of hypersensitivity to isoniazid, niacin, pyrazinamide, or chemically related ; these ptients also may be hypersensitive to ethionamide.

Expect to give another antituberculotic with ethionamide to decrease the risk of development of bacterial resistance.

Also plan to give pyridoxine to prevent or minimize peripheral neuritis (burning, numbness, pain, or tingling in hands and feet), especially if patient has already had isoniazid-induced peripheral neuritis.

Monitor liver function test results, and assess for signs of impaired function, such as hepatitis and jaundice.

Question patient regularly about vision changes. Notify prescriber about blurred vision, eye pain, or loss of vision or acuity.

Monitor compliance; treatment may need to continue for 1 to 2 years or indefinitely.

PATIENT SAFTY

Advise patient to take ethionamide with food if adverse GI reactions occur.

Instruct patient to take a missed dose as soon as he remembers unless it’s nearly time for the next dose. Caution him not to double the dose.

Encourage patient to notify prescriber if no improvement occurs within 3 weeks; if bothersome or severe

Side Efect

occur; if his vision changes; or if he has burning, numbness, pain, or tingling in his hands and feet.

Inform patient that therapy may have to continue for months or years and that compliance is essential.

Category

Chemical class: Succinimide derivative
Therapeutic class: Anticonvulsant

Pregnancy category: Not rated

Indications

To manage absence seizures in a patient who also has generalized tonic-clonic seizures , SYRUP Adults and children age 6 and over. Initial: 500 mg daily. Maintenance: Increased by 250 mg every 4 to 7 days until control is achieved with minimal

Side Efect

. Children ages 3 to 6. Initial: 250 mg daily. Maintenance: Increased by 250 mg every 4 to 7 days until control is achieved with minimal

Side Efect

.

Mechanism of Action

Elevates the seizure threshold and reduces the frequency of attacks by depressing the motor cortex and elevating the threshold of CNS response to convulsive stimuli.

Contraindications

Hypersensitivity to ethosuximide, succinimides, or their components

Interactions

carbamazepine, phenobarbital, phenytoin, primidone: Possibly decreased blood ethosuximide level
CNS depressants: Possibly increased CNS depression
haloperidol: Possibly decreased blood haloperidol level ethosuximide 412 loxapine, MAO inhibitors, maprotiline, molindone, phenothiazines, pimozide, tricyclic antidepressants: Possibly lowered seizure threshold and reduced therapeutic effect of ethosuximide
valproic acid: Increased or decreased blood ethosuximide level
alcohol use: Possibly increased CNS depression

Side Efect

CNS: Aggressiveness, ataxia, decreased concentration, dizziness, drowsiness, euphoria, fatigue, headache, hyperactivity, irritability, lethargy, nightmares, sleep disturbance, suicidal ideation
EENT: Gingival hypertrophy, myopia, tongue swelling
GI: Abdominal and epigastric pain, abdominal cramps, anorexia, diarrhea, hiccups, indigestion, nausea, vomiting
GU: Increased libido, microscopic hematuria, vaginal bleeding
HEME: Agranulocytosis, aplastic anemia, eosinophilia, leukopenia, pancytopenia
SKIN: Erythematous and pruritic rash, hirsutism, Stevens-Johnson syndrome, systemic lupus erythematosus, urticaria
Other: Hypersensitivity reaction, weight loss

Cautions

Use ethosuximide with extreme caution in patients with hepatic or renal disease.

Give other anticonvulsants concurrently, as prescribed, to control generalized tonicclonic seizures.

Monitor CBC and platelet count and assess for signs of infection, such as cough, fever, and pharyngitis. Also routinely evaluate liver and renal function test results.

Take safety precautions because drug may cause adverse CNS reactions, such as dizziness and drowsiness.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

PATIENT SAFTY

Stress the importance of complying with ethosuximide regimen.

Advise patient to take a missed dose as soon as he remembers unless it’s nearly time for the next dose. Warn him not to double the dose.

Instruct patient not to engage in potentially hazardous activities until drug’s CNS effects are known.

Caution patient not to stop taking drug abruptly; doing so increases the risk of absence seizures.

Urge caregivers to watch patient closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes, and to report any concerns immediately to prescriber.

Encourage female patient who becomes pregnant while taking ethosuximide to enroll in the North American antiepileptic drug pregnancy registry by calling 1-888233-2334. Explain that this registry is collecting information about the safety of antiepileptic during pregnancy.

Category

Chemical class: Hydantoin derivative
Therapeutic class: Anticonvulsant

Pregnancy category: D

Indications

To treat tonic-clonic and simple or complex partial seizures as initial or adjunct therapy, or when other are ineffective Adults and adolescents. Initial: 0.5 to 1 g on the first day in four to six divided doses, increased over several days until desired response is reached. Maintenance: 2 to 3 g daily in four to six divided doses. Maximum: 3 g daily. Children. Initial: Up to 750 mg daily, based on weight and age, in 4 to 6 divided doses, adjusted as needed and tolerated. Maintenance: 0.5 to 1 g daily in 4 to 6 divided doses. Maximum: 3 g daily.
DOSAGE ADJUSTMENT For debilitated patients, initial dosage lowered to reduce the risk of

Side Efect

.

Mechanism of Action

Limits the spread of seizure activity and the start of new seizures by:

regulating voltage-dependent sodium and calcium channels in neurons ethotoin 413 E F

inhibiting calcium movement across neuronal membranes

enhancing sodium-potassium adenosine triphosphatase activity in neurons and glial cells. These actions may result from ethotoin’s ability to slow the recovery rate of inactivated sodium channels.

Contraindications

Hematologic disorders; hepatic dysfunction; hypersensitivity to ethotoin, phenytoin, other hydantoins, or their components

Interactions

acetaminophen: Increased risk of hepatotoxicity with long-term acetaminophen use amiodarone: Possibly increased blood ethotoin level and risk of toxicity antacids: Possibly decreased ethotoin effectiveness bupropion, clozapine, loxapine, MAO inhibitors, maprotiline, phenothiazines, pimozide,
thioxanthenes: Possibly lowered seizure threshold and decreased therapeutic effects of ethotoin; possibly intensified CNS depressant effects of these chloramphenicol, cimetidine, disulfiram, fluconazole, isoniazid, methylphenidate, metronidazole, omeprazole, phenylbutazone, ranitidine, salicylates, sulfonamides, trimethoprim: Possibly impaired metabolism of these and increased risk of ethotoin toxicity corticosteroids, cyclosporine, digoxin, disopyramide, doxycycline, furosemide, levodopa, mexiletine,
quinidine: Decreased therapeutic effects of these diazoxide: Possibly decreased therapeutic effects of both estrogens, progestins: Decreased effects of these , increased blood ethotoin level folic acid, leucovorin: Increased ethotoin metabolism, decreased seizure control
haloperidol: Possibly lowered seizure threshold, decreased ethotoin effects, and decreased blood haloperidol level insulin, oral antidiabetic : Possibly increased blood glucose level and decreased therapeutic effects of these lidocaine: Increased lidocaine metabolism, leading to reduced concentration methadone: Possibly increased methadone metabolism and withdrawal symptoms molindone: Possibly lowered seizure threshold and impaired absorption and decreased therapeutic effects of ethotoin oral anticoagulants: Possibly impaired metabolism of these and increased risk of ethotoin toxicity; possibly increased anticoagulant effect initially, but decreased effect with prolonged therapy oral contraceptives that contain estrogen and progestin: Possibly breakthrough bleeding and decreased contraceptive effectiveness
rifampin: Possibly decreased therapeutic effects of ethotoin streptozocin: Possibly decreased therapeutic effects of streptozocin sucralfate: Possibly decreased ethotoin absorption tricyclic antidepressants: Possibly lowered seizure threshold and decreased therapeutic effects of ethotoin; possibly decreased blood level of tricyclic antidepressants
valproic acid: Possibly decreased ethotoin level, increased valproic acid level vitamin D analogues: Decreased vitamin D analogue activity; risk of anticonvulsantinduced rickets and osteomalacia xanthines: Possibly inhibited ethotoin absorption and increased clearance of xanthines
alcohol use: Possibly decreased ethotoin effectiveness, increased CNS depression

Side Efect

CNS: Clumsiness, confusion, drowsiness, excitement, peripheral neuropathy, sedation, slurred speech, stuttering, suicidal ideation, tremor
EENT: Nystagmus
GI: Constipation, diarrhea, nausea, vomiting
HEME: Agranulocytosis, leukopenia, thrombocytopenia
SKIN: Rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Lymphadenopathy, systemic lupus erythematosus

Cautions

Obtain CBC and differential before treatment and monthly for first few months of ethotoin therapy, as ordered.
WARNING Ethotoin shouldn’t be stopped abruptly because of risk of status epilepticus. Plan to reduce dosage gradually or substitute another drug, as prescribed. ethotoin 414

Monitor patient for signs and symptoms of infection or unusual bleeding because ethotoin may cause hematologic toxicity.

Because of ethotoin’s potential for hepatotoxicity, monitor liver function test results and expect drug to be discontinued if test results are abnormal.

Notify prescriber immediately and expect ethotoin to be stopped and replaced with another drug if patient has decreased blood counts, enlarged lymph nodes, or rash.

Be aware that ethotoin may be substituted for phenytoin without loss of seizure control if patient develops severe gingival hyperplasia or other

Side Efect

. Expect ethotoin dosage to be 4 to 6 times greater than phenytoin dosage.

Institute and maintain seizure precautions according to facility protocol.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

PATIENT SAFTY

Instruct patient to take ethotoin exactly as prescribed and not to stop it abruptly.

Advise patient to take drug with food to enhance absorption and reduce adverse GI effects.

Advise patient to report easy bruising, epistaxis, fever, malaise, petechiae, or sore throat to prescriber immediately.

Instruct patient to keep medical appointments to monitor drug effectiveness and check for

Side Efect

. Explain the need for periodic laboratory tests.

Urge patient to avoid alcohol during ethotoin therapy.

Caution patient to avoid hazardous activities until drug’s adverse effects are known.

Encourage patient to wear or carry medical identification indicating his diagnosis and drug therapy.

Urge caregivers to watch patient closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes, and to report any concerns immediately to prescriber.

Encourage female patient who becomes pregnant while taking ethotoin to enroll in the North American antiepileptic drug pregnancy registry by calling 1-888-2332334. Explain that this registry is collecting information about the safety of antiepileptic during pregnancy.

Category

Chemical class: Bisphosphonate
Therapeutic class: Antihypercalcemic agent, bone resorption inhibitor

Pregnancy category: B

(oral), C (parenteral)

Indications

To treat Paget’s disease of bone (osteitis deformans)
Adults.5 to 10 mg/kg daily for up to 6 mo, or 11 to 20 mg/kg daily for up to 3 mo. To prevent and treat heterotopic ossification after total hip replacement
Adults. 20 mg/kg daily for 1 mo before surgery and then 20 mg/kg daily for 3 mo after surgery for a total of 4 mo of treatment. To prevent and treat heterotopic ossification after spinal cord injury
Adults. 20 mg/kg daily for 2 wk and then 10 mg/kg daily for 10 wk for a total of 12 wk of treatment. To treat moderate to severe hypercalcemia caused by cancer
IV:
Adults. Initial: 7.5 mg/kg daily infused over at least 2 hr for 3 to 7 successive days. Oral etidronate may begin at 20 mg/kg/day for 30 days on the day after last infusion.
DOSAGE ADJUSTMENT Dosage reduced in renal impairment. Drug not given if serum creatinine level exceeds 5 mg/dl.

Mechanism of Action

Inhibits normal and abnormal bone resorption by reducing bone turnover and slowing the remodeling of pagetic or heterotopic bone. Etidronate also decreases the elevated cardiac output seen in Paget’s disease of bone and reduces local increases in skin temperature. It also inhibits the abnormal bone resorption that may occur with cancer and reduces the amount of calcium that enters the blood from resorbed bone.

Contraindications

Esophageal abnormalities that delay gastric emptying, such as achalasia and stricture; hypersensitivity to etidronate, bisphosphoetidronate disodium 415 E F nates, or their components; severe renal impairment

Interactions

antacids that contain aluminum, calcium, or magnesium; vitamin and mineral supplements that contain aluminum, calcium, iron, or magnesium: Decreased etidronate absorption high-calcium food (such as milk and other dairy products): Decreased etidronate absorption

Side Efect

EENT: Altered taste, metallic taste
GI: Diarrhea, elevated liver function test results, nausea
GU: Nephrotoxicity
MS: Bone fractures, bone pain, osteonecrosis of jaw
Other: Hypocalcemia

Cautions

Use etidronate cautiously in patients with upper GI problems such as Barrett’s esophagus, dysphagia, other esophageal diseases, gastritis, duodenitis, or ulcers because drug may cause local irritation of the upper GI mucosa.

Anticipate starting etidronate as soon as possible after spinal cord injury, preferably before signs of heterotopic ossification.

Expect etidronate not to inhibit healing of spinal fractures, affect prosthesis, or disrupt trochanter attachment when used after total hip replacement.

Give oral form 2 hours before meals to prevent decreased absorption.

Dilute parenteral form in at least 250 ml of normal saline solution.

Give parenteral form slowly over at least 2 hours.

Store diluted parenteral solution at room temperature for up to 48 hours.
WARNING Watch for hypocalcemia if patient receives parenteral form for more than 3 days.

When treating hypercalcemia, expect to continue giving drug for up to 90 days if serum calcium level remains within acceptable range.

Monitor patient for adverse esophageal effects such as esophagitis, esophageal ulcers, and esophageal erosions that may occur with bleeding, as well as gastric and duodenal ulcers, because these adverse effects have occurred with other oral biphosphonates.

Risk of severe adverse esophageal reactions increases in patients who lie down after taking drug, who fail to swallow it with a full glass of water, or who continue to take drug after developing symptoms of esophageal irritation.

Make sure patient has had a dental checkup before having an invasive dental procedures during etidronate therapy, especially if he has cancer; is receiving chemotherapy, head or neck radiation, or a corticosteroid; or has poor oral hygiene because the risk of osteonecrosis is increased in these patients.

PATIENT SAFTY

Instruct patient to take etidronate tablets on an empty stomach—2 hours before meals, antacids, or calcium supplements. Urge him to drink a full glass of water with tablets and to avoid taking drug with milk or other high-calcium

Tell patient to take a missed dose as soon as he remembers as long as 2 hours have elapsed since his last meal. Instruct him not to eat for another 2 hours. Warn against doubling the dose.

Inform patient with Paget’s disease that his response to etidronate may be slow and may continue for months after treatment.

Category

Chemical class: Pyranoindoleacetic acid derivative
Therapeutic class: Analgesic, antiinflammatory

Pregnancy category: C

Indications

To manage osteoarthritis ,
Adults. Initial: 800 to 1,200 mg daily in divided doses. Maintenance: 600 to 1,200 mg daily in divided doses. Maximum: 1,200 mg daily for patients weighing 60 kg (132 lb) or more; 20 mg/kg daily for those less than 60 kg. etodolac 416
Adults. 400 to 1,000 mg daily. To relieve mild to moderate pain ,
Adults.Initial: 400 mg and then 200 to 400 mg every 6 to 8 hr. Maximum: 1,200 mg daily for patients weighing 60 kg or more; 20 mg/kg/day for patients weighing less than 60 kg. Route Onset Peak Duration P.O. 30 min 1–2 hr 4–12 hr

Mechanism of Action

Blocks the activity of cyclooxygenase, the enzyme needed for prostaglandin synthesis. Prostaglandins, important mediators of the inflammatory response, cause local vasodilation with swelling and pain. By inhibiting cyclooxygenase and prostaglandins, this NSAID causes inflammatory symptoms and pain to subside.

Contraindications

Angioedema, asthma, bronchospasm, nasal polyps, rhinitis, or urticaria induced by aspirin, iodides, or NSAIDs; coronary artery bypass graft surgery; hypersensitivity to etodolac or its components

Interactions

ACE inhibitors: Possibly decreased hypotensive effects of these acetaminophen (long-term use): Increased risk of adverse renal effects antacids: Decreased blood etodolac level antiplatelets, oral anticoagulants, thrombolytics: Prolonged PT (with warfarin), increased risk of bleeding cidofovir: Possibly nephrotoxicity corticosteroids: Increased risk of adverse GI effects cyclosporine: Increased nephrotoxic effects, increased blood cyclosporine level digoxin: Increased blood digoxin level and risk of digitalis toxicity insulin, oral antidiabetic : Increased risk of hypoglycemia lithium: Increased blood lithium level and, possibly, toxicity loop diuretics: Possibly decreased effects of loop diuretics methotrexate: Increased risk of methotrexate toxicity phenylbutazone: Possibly altered etodolac clearance salicylates: Decreased blood etodolac level, increased risk of adverse GI effects
warfarin: Synergistic bleeding effects alcohol use, smoking: Increased risk of adverse GI effects

Side Efect

CNS: Asthenia, chills, depression, dizziness, drowsiness, fatigue, fever, insomnia, irritability, malaise, nervousness, seizures, somnolence, syncope, stroke
CV: Edema, heart failure, hypertension, MI, palpitations, tachycardia, vasculitis
EENT: Blurred vision, deafness, loss of taste, photophobia, tinnitus
ENDO: Hyperglycemia in diabetics
GI: Abdominal pain or distention, anorexia, constipation, diarrhea, diverticulitis, dyspepsia, dysphagia, elevated liver function test results, esophagitis, flatulence, gastritis, gastroenteritis, gastroesophageal reflux disease, GI bleeding and ulceration, GI perforation, hemorrhoids, hepatic failure, hepatitis, hiatal hernia, indigestion, melena, nausea, pancreatitis, peptic ulcer, perforation of stomach or intestines, stomatitis, vomiting
GU: Dysuria, elevated serum creatinine level, hematuria, renal failure or insufficiency, renal papillary necrosis, urinary frequency
HEME: Agranulocytosis, aplastic anemia, easy bruising, hemolytic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia
MS: Arthralgia, muscle pain
RESP: Asthma, bronchospasm, pulmonary infiltrate with eosinophilia, respiratory depression
SKIN: Erythema multiforme, exfoliative dermatitis, flushing, leukocytoclastic vasculitis, pruritus, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria, vesiculobullous or other rash
Other: Anaphylaxis, angioedema, lymphadenopathy, sepsis

Cautions

Assess patient’s hydration status and rehydrate, if needed and as ordered, before starting etodolac therapy.

Use etodolac with extreme caution in patients with a history of ulcer disease or GI bleeding because NSAIDs increase the etodolac 417 E F risk of GI bleeding and ulceration. Expect to use etodolac for the shortest time possible in these patients. Also use with extreme caution in patients with advanced renal disease because etodolac is eliminated mainly by the kidneys.

Be aware that serious GI tract ulceration, bleeding, and perforation may occur without
WARNING symptoms. Elderly patents are at greater risk. To minimize risk, give drug with food. If GI distress occurs, withhold drug and notify prescriber immediately.

Use etodolac cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.
WARNING Monitor patient closely for thrombotic events, including stroke and MI, because NSAIDs increase the risk.

Especially if patient is elderly or taking etodolac long-term, watch for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results. Rarely, elevated levels may progress to severe hepatic reactions, including fatal hepatitis, hepatic necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in patients with heart failure, hepatic dysfunction, or impaired renal function; those taking diuretics or ACE inhibitors; and elderly patients because drug may cause renal failure.

Monitor CBC for decreased hemoglobin level and hematocrit because drug may worsen anemia.
WARNING If patient has bone marrow suppression or is receiving antineoplastic drug therapy, monitor laboratory results (including WBC count), and watch for evidence of infection because anti-inflammatory and antipyretic actions of etodolac may mask it, such as fever and pain.

Assess patient’s skin routinely for rash or other signs of hypersensitivity reaction because etodolac and other NSAIDs may cause serious skin reactions without warning, even in patients with no history of NSAID hypersensitivity Stop drug at first sign of reaction and notify prescriber.

If patient also takes acetaminophen, monitor fluid intake and output and BUN and serum creatinine levels for signs of adverse renal reactions.

PATIENT SAFTY

Tell patient to take etodolac with food or after meals if adverse GI reactions occur.

Caution him to avoid aspirin or aspirincontaining products while taking drug.

Advise patient not to smoke or drink alcohol during therapy because these activities increase the risk of adverse GI reactions.

Inform patient that he may experience dizziness or drowsiness.

Instruct him to notify prescriber immediately about blood in urine, easy bruising, itching, rash, swelling, or yellow eyes or skin.

Caution pregnant patient not to take etodolac or other NSAIDs during the third trimester because drug may cause premature closure of the ductus arteriosus.

Explain that etodolac may increase the risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention for possible reactions, chest pain, shortness of breath, weakness, and slurring of speech.

Tell patient that etodolac therapy also may increase the risk of serious adverse GI reactions; stress the importance of seeking immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.

Explain the possibility of rare but serious skin reactions. Urge patient to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity.

Category

Chemical class: Amino acid peptide amide
Therapeutic class: Antidiabetic drug

Pregnancy category: C

Indications

Adjunct treatment to improve blood gluexenatide 418 cose levels in patients with type 2 diabetes mellitus who are taking metformin, a sulfonylurea, a thiazolidinedione, or a combination of metformin and a sulfonylurea or metformin and a thiazolidinedione but have not achieved adequate glucose control SUBCUTANEOUS INJECTION
Adults.Initial: 5 mcg b.i.d., given within 60 min before morning and evening meals. After 1 mo, increased as needed to 10 mcg b.i.d., given within 60 min before morning and evening meals. Adjunct treatment to diet and exercise to improve blood glucose levels in patients with type 2 diabetes mellitus SUBCUTANEOUS INJECTION
Adults.Initial: 5 mcg b.i.d., given within 60 min before morning and evening meals. After 1 mo, increased as needed to 10 mcg b.i.d., given within 60 min before morning and evening meals. Route Onset Peak Duration SubQ Immediate 2.1 hr Unknown

Contraindications

Hypersensitivity to exenatide or its components, ketoacidosis, type 1 diabetes mellitus

Interactions

oral antidiabetics: Increased risk of hypoglycemia oral : May decrease rate and extent of absorption of these
warfarin: Possibly increased INR with increased risk of bleeding

Side Efect

CNS: Asthenia, dizziness, headache, jitteriness, somnolence
CV: Chest pain
EENT: Decreased taste
ENDO: Hypoglycemia
GI: Abdominal distention or pain, anorexia, constipation, diarrhea, dyspepsia, flatulence, gastroesophageal reflux, indigestion, nausea, pancreatitis (including life-threatening hemorrhagic or necrotizing), vomiting
GU: Decreased renal function
RESP: Chronic hypersensitivity pneumonitis
SKIN: Diaphoresis, pruritus, rash, urticaria
Other: Anaphylaxis, angioedema, antiexenatide antibodies, dehydration, elevated anti-exenatide antibody level, injection site reactions, weight loss

Cautions

Exenatide isn’t recommended for patients exenatide 419 E F Absorbed into bloodstream Food ingested Exenatide injected Liver: glucose output decreased Small intestine: glucose absorption slowed Pancreas: insulin output increased Normally, when serum glucose level rises, insulin is secreted within 10 minutes. This first-phase insulin response is absent in patients with type 2 diabetes. Exenatide, an incretin mimetic, restores the first-phase insulin response and improves the second

Mechanism of Action

phase response that immediately follows. It does so by promoting incretins that spur insulin synthesis and release from beta cells by binding and activating human GLP-1 receptors to reduce fasting and postprandial serum glucose levels. The drug also suppresses inappropriately elevated glucagon secretion. Lower serum glucagon level leads to decreased hepatic glucose output and decreased insulin demand. It also slows gastric emptying and thus the rise of serum glucose level. with severe GI disease, patients with creatinine clearance less than 30 ml/ min/ 1.73 m2, or patients having dialysis because of adverse GI or renal effects.

Use exenatide cautiously in a renal transplant patient or patient with moderate renal disease when dosage is increased from 5 mcg to 10 mcg. Monitor renal function throughout therapy, and notify prescriber of abnormalities.

If patient also takes a sulfonylurea, the sulfonylurea dosage may need to be decreased to reduce the risk of hypoglycemia. Usually, no
DOSAGE ADJUSTMENT is needed for a patient taking metformin.

Administer drug into patient’s thigh, abdomen, or upper arm.

Monitor patient’s blood glucose level. If control decreases despite the patient’s best efforts, drug may need to be discontinued because of the possibility that anti-exenatide antibodies have formed.

Monitor patient for evidence of acute pancreatitis, such as persistent, severe abdominal pain accompanied by vomiting, especiially when drug is started or dosage increased. Notify prescriber, and expect to stop exenatide and give supportive care.

PATIENT SAFTY

Teach patient how to give a subcutaneous injection and how to use pen injector.

Inform patient that exenatide may be administered in the thigh, abdomen, or upper arm. Stress the need to rotate injection sites.

Stress the need to use drug within 60 minutes before morning and evening meals or the two main meals of the day, about 6 hours or more apart, never after a meal.

If patient misses a dose, tell him to resume treatment with the next scheduled dose.

Advise patient that drug should look clear and colorless. Caution against using prefilled pen device in which solution looks cloudy or colored or contains particles.

Instruct patient to check expiration date on the vial and not to use drug if date has passed.

Advise patient to refrigerate drug before first use and protect it from light. After first use, drug may be stored at room temperature of 77° F (25° C) or less.

Tell patient to discard pen injector 30 days after initial use, even if some drug is left.

Alert patient that pen doesn’t come with needles and that he’ll need to buy them.

Warn patient that nausea may occur at the beginning of therapy.

Inform patient taking a sulfonylurea to be alert for hypoglycemic reactions because risk increases with both . Review ways to treat such reactions, and tell patient to alert prescriber if they occur often or are severe.

Instruct female patient of childbearing potential to tell her prescriber if she is, could be, or is planning to become pregnant.

Tell patient to seek emergency care for persistent, severe abdominal pain and vomiting.

Caution patient that exenatide doesn’t replace diet and exercise measures.

Category

Chemical class: Azetidinone
Therapeutic class: Antihypercholesterolemic

Pregnancy category: C

Indications

To treat heterozygous familial and nonfamilial hypercholesterolemia or homozygous sitosterolemia; as adjunct with HMG-CoA reductase inhibitors to treat heterozygous familial and nonfamilial hypercholesterolemia; with fenofibrate to treat mixed hyperlipidemia and with atorvastatin or simvastatin to treat patients with homozygous familial hypercholesterolemia
Adults.10 mg daily.

Contraindications

Active hepatic dysfunction, hypersensitivity to ezetimibe or its components

Interactions

cholestyramine: Reduced effects of ezetimibe cyclosporine: Increased blood cyclosporine and ezetimibe levels fenofibrate, gemfibrozil: Increased blood ezetimibe level ezetimibe 420

Side Efect

CNS: Depression, dizziness, fatigue, headache, paresthesia
CV: Chest pain
EENT: Pharyngitis, sinusitis
GI: Abdominal pain, cholelithiasis, cholecystitis, diarrhea, elevated liver function test results, hepatitis, nausea, pancreatitis
HEME: Thrombocytopenia
MS: Arthralgia, back or limb pain, elevated CK level, myalgia, myopathy, rhabdomyolysis
RESP: Cough, upper respiratory tract infection
SKIN: Erythema multiforme, rash, urticaria
Other: Anaphylaxis, angioedema, influenza, viral infection

Cautions

Monitor liver function test results before and during ezetimibe therapy, as ordered.

Know that you should give ezetimibe 2 hours before or 4 hours after giving bile acid sequestrant, cholestyramine, or colestipol.

PATIENT SAFTY

Direct patient to follow a low-cholesterol diet as an adjunct to ezetimibe therapy. Recommend weight loss and exercise programs, as appropriate.

If patient also takes a bile acid sequestrant, tell him to take ezetimibe either 2 hours before or at least 4 hours after it to prevent drug interactions.

Advise patient to report unexplained muscle pain, tenderness, or weakness.

Category

Chemical class: Thiazole derivative
Therapeutic class: Antiulcer agent, gastric acid secretion inhibitor

Pregnancy category: B

Indications

To provide short-term treatment of famotidine 421 E F

Mechanism of Action

Reduces blood cholesterol by inhibiting its absorption through the small intestine. Normally, in the intestinal lumen, lipids break down to cholesterol and other substances that create smaller droplets called micelles, as shown below left. The micelles enter intestinal epithelial cells called enterocytes, where they combine with triglycerides, cholesterol, and other substances to form chylomicrons. Chylomicrons then pass through to the lymphatic system to be carried to the blood. Ezetimibe blocks cholesterol absorption into enterocytes and keeps cholesterol from moving through the intestinal wall, as shown below right. Reduced cholesterol absorption from the intestine decreases chylomicron and LDL cholesterol content. active duodenal ulcer ORAL SUSPENSION,(CHEWABLE, ORAL DISINTEGRATING, AND REGULAR) Adults and adolescents.40 mg daily at bedtime or 20 mg b.i.d. Children.0.5 mg/kg daily as a single dose at bedtime or in divided doses b.i.d.
IV: OR INJECTION Adults and adolescents over age 16. 20 mg every 12 hr, infused over 15 to 30 min or injected over at least 2 min. Children ages 1 to 16. Initial: 0.25 mg/kg every 12 hr, infused over 15 to 30 min or injected over at least 2 min. Maximum: 40 mg daily. To prevent recurrence of duodenal ulcer ORAL SUSPENSION,(CHEWABLE, ORAL DISINTEGRATING, AND REGULAR) Adults and adolescents. 20 mg daily at bedtime. To provide short-term treatment for active, benign gastric ulcer ORAL SUSPENSION,(CHEWABLE, ORAL DISINTEGRATING, AND REGULAR) Adults and adolescents.40 mg daily at bedtime. Children.0.5 mg/kg daily as a single dose at bedtime or in divided doses b.i.d.
IV: OR INJECTION Adults and adolescents over age 16. 20 mg every 12 hr. Children ages 1 to 16. Initial: 0.25 mg/kg every 12 hr. Maximum: 40 mg daily. To treat gastroesophageal reflux disease (GERD) ORAL SUSPENSION,(CHEWABLE, ORAL DISINTEGRATING, AND REGULAR) Adults and adolescents.20 mg b.i.d. for up to 6 wk. Children weighing more than 10 kg (22 lb). 1 to 2 mg/kg daily in divided doses b.i.d. Children weighing less than 10 kg. 1 to 2 mg/kg daily in divided doses t.i.d. ORAL SUSPENSION Infants age 4 months to 1 year.0.5 mg/kg daily in divided doses b.i.d. for up to 8 wk. Infants age 3 months or less. 0.5 mg/kg daily for up to 8 wk.
IV: OR INJECTION Children ages 1 to 16. Initial: 0.25 mg/kg every 12 hr. Maximum: 40 mg daily. To treat esophagitis caused by gastroesophageal reflux ORAL SUSPENSION,(CHEWABLE, ORAL DISINTEGRATING, AND REGULAR) Adults and adolescents.20 to 40 mg b.i.d. for up to 12 wk. To treat gastric hypersecretory conditions, such as Zollinger-Ellison syndrome ORAL SUSPENSION,(CHEWABLE, ORAL DISINTEGRATING, AND REGULAR) Adults and adolescents. Initial: 20 mg every 6 hr. Dosage adjusted, if needed, based on patient response.
IV: OR INJECTION Adults and adolescents.20 mg every 12 hr. To prevent heartburn and indigestion (CHEWABLE, ORAL DISINTEGRATING, AND REGULAR) Adults and adolescents.10 mg 1 hr before eating. Maximum: 20 mg every 24 hr. To treat heartburn and indigestion (CHEWABLE, ORAL DISINTEGRATING, AND REGULAR) Adults and adolescents.10 mg at onset of symptoms. Maximum: 20 mg every 24 hr for up to 2 wk unless prescribed otherwise.
DOSAGE ADJUSTMENT Oral or parenteral dosage reduced or dosing interval increased (to 36 to 48 hr), if needed, in patients with renal insufficiency and creatinine clearance of 49 ml/min/1.73 m2or less. Route Onset Peak Duration P.O. 1 hr 1–4 hr 10–12 hr I.V. In 30 min 0.5–3 hr 10–12 hr

Contraindications

Hypersensitivity to famotidine, other H2receptor antagonists, or their components

Interactions

antacids, sucralfate: Possibly decreased absorption of famotidine bone marrow depressants: Increased risk of blood dyscrasias itraconazole,
ketoconazole: Possibly decreased absorption of these
alcohol use: Possibly increased blood alcohol level

Side Efect

CNS: Agitation (infants), anxiety, asthenia, confusion, depression, dizziness, fatigue, fever, hallucinations, headache, insomnia, famotidine 422 mental or mood changes, paresthesia, seizures, somnolence
CV: Arrhythmias, AV block, palpitations
EENT: Dry mouth, laryngeal edema, taste alteration, tinnitus
GI: Abdominal pain, anorexia, cholestatic jaundice, constipation, diarrhea, elevated liver enzymes, hepatitis, nausea, vomiting
GU: Decreased libido
HEME: Agranulocytosis, aplastic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia
MS: Arthralgia, muscle cramps
RESP: Bronchospasm, dyspnea, interstitial pneumonia, wheezing
SKIN: Acne, alopecia, dry skin, erythema multiforme, exfoliative dermatitis, flushing, jaundice, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, facial edema, hyperuricemia

Cautions

Shake famotidine oral suspension vigorously for 5 to 10 seconds before administration.

Dilute injection form (2 ml) with normal saline solution or other solution to 5 to 10 ml; give I.V. injection over at least 2 minutes. Or dilute in 100 ml of D5W and infuse over 15 to 30 minutes. Or infuse premixed injection (20 mg/50 ml normal saline solution) over 15 to 30 minutes.
WARNING Be aware that Pepcid AC chewable tablets contain aspartame, which can be dangerous for patients who have phenylketonuria.

PATIENT SAFTY

Instruct patient to store famotidine oral suspension at room temperature (below 86° F [30° C]) and to protect it from freezing. Tell her to shake the bottle vigorously for 5 to 10 seconds after adding water and right before use.

Advise patient who uses Pepcid RPD to store drug in unopened package. For each dose, instruct her to open blister pack with dry hands, place a tablet on her tongue, let it dissolve, and swallow it with saliva.

If patient uses chewable tablets, instruct her to chew them thoroughly before swallowing.

If patient also takes antacids, instruct her to wait 30 to 60 minutes after taking famotidine, if possible, before taking antacid.

Caution patient to avoid alcohol and smoking during famotidine therapy because they irritate the stomach and can delay ulcer healing.

Advise patient to notify prescriber if she famotidine 423 E F

Mechanism of Action

In normal digestion, parietal cells in the gastric epithelium secrete hydrogen (H+) ions, which combine with chloride ions (Cl–) to form hydrochloric acid (HCl), as shown below left. However, HCl can inflame, ulcerate, and perforate gastric and intestinal mucosa normally protected by mucus. Famotidine, an H2-receptor antagonist, reduces HCl formation by preventing histamine from binding with H2receptors on the surface of parietal cells, as shown below right. By doing so, drug helps prevent peptic ulcers from forming and helps heal existing ones. Parietal cell Histamine HCl H+ ClH2 receptor Histamine Famotidine Parietal cell Histamine HCl H+ ClH2 receptor Histamine Famotidine develops pain or has trouble swallowing or if she has bloody vomit or black stools.

Caution patient not to take famotidine with other acid-reducing products.

Category

Chemical class: Non-purine xanthine oxidase inhibitor
Therapeutic class: Antigout

Pregnancy category: C

Indications

To treat chronic hyperuricemia in patients with gout
Adults. Initial: 40 mg once daily, increased after 2 wk to 80 mg once daily, if needed. Route Onset Peak Duration P.O. 2–3 days 1–1.5 hr Unknown

Mechanism of Action

Inhibits the action of xanthine oxidase, the key enzyme responsible for purine breakdown. Xanthine oxidase catalyzes conversion of xanthine to uric acid, thereby increasing uric acid levels. High uric acid levels cause gout attacks. Inhibiting xanthine oxidase causes uric acid levels to drop, decreasing the risk of gout attack.

Contraindications

Concurrent use of azathioprine, mercaptopurine, or theophylline; hypersensitivity to febuxostat or its components

Interactions

azathioprine, mercaptopurine,
theophylline: Possibly increased serum levels of these , leading to toxicity

Side Efect

CNS: Dizziness, hemiparesis, lacunar infarction, stroke, transient ischemic attack
CV: Angina, chest pain or discomfort, ECG abnormalities, MI
EENT: Blurred vision, deafness, epistaxis, nasal dryness, paranasal sinus hypersecretion, pharyngeal edema, sneezing, taste disturbance, throat irritation, tinnitus
ENDO: Breast pain, gynecomastia, hot flashes, hypoglycemia
GI: Diarrhea, dyspepsia, GI discomfort, hepatomegaly, liver function abnormalities, nausea, vomiting
GU: Decreased libido, erectile dysfunction, hematuria, nephrolithiasis, pollakiuria, proteinuria, renal failure or insufficiency, urgency
HEME: Anemia, idiopathic thrombocytopenic purpura, leukocytosis, leukopenia, neutropenia, pancytopenia, splenomegaly, thrombocytopenia
MS: Arthralgia, joint stiffness or swelling
RESP: Upper respiratory tract infection
SKIN: Dermatitis, ecchymosis, eczema, flushing, hair color or growth changes, hyperhidrosis, peeling skin, petechiae, photosensitivity, rash
Other: Gout flares, hypersensitivity

Cautions

Febuxostat therapy isn’t recommended for patients in whom rate of urate formation is greatly increased, as in malignancy and its treatment or Lesch-Nyhan syndrome.

Monitor patient’s serum uric acid level, as prescribed, to determine drug effectiveness. Expect it to take about 2 weeks for uric acid level to be therapeutically altered. Dose may be increased from 40 mg to 80 mg daily if target serum uric acid level fails to fall below 6 mg/dl.

Monitor patient for gout flares, which may occur after therapy is started because of changing serum uric acid levels that result in mobilization of urate from tissue deposits. Expect prescriber to order an NSAID or colchicine when febuxostat therapy starts. If patient has a gout flareup during treatment, notify prescriber, and expect symptoms to be managed. Know that febuxostat therapy usually isn’t discontinued during this time.

Monitor patient for evidence of cardiovascular thrombosis, such as acute MI or stroke, because drug may increase patient’s risk of developing these disorders.

Monitor patient’s liver enzyme levels, as ordered, especially 2 and 4 months after therapy starts and periodically thereafter.

PATIENT SAFTY

Inform patient that a gout attack may occur when febuxostat therapy starts and febuxostat 424 that NSAIDs or colchicine may be prescribed, usually along with febuxostat, to prevent it.

Instruct patient to seek emergency care immediately for signs or symptoms of a heart attack or stroke.

Tell patient that periodic blood tests will be needed to determine drug’s effectiveness and to detect adverse effects.

Category

Chemical class: Dicarbamate
Therapeutic class: Anticonvulsant

Pregnancy category: C

Indications

To treat partial seizures in patients who don’t respond to other ORAL SUSPENSION, Adults and adolescents over age 14. Initial: 1,200 mg daily in divided doses t.i.d. or q.i.d. Dosage increased over several weeks based on patient response. Maximum: 3,600 mg daily. Children ages 2 to 14. Initial: 15 mg/kg daily in divided doses t.i.d. or q.i.d. Dosage increased over several weeks based on patient response. Maximum: 3,600 mg daily or 45 mg/kg daily. As adjunct to treat generalized or partial seizures associated with Lennox-Gastaut syndrome in children ORAL SUSPENSION, Children ages 2 to 14. Initial: 15 mg/kg daily in divided doses t.i.d. or q.i.d. while decreasing other anticonvulsant by 20% to control their blood levels. Felbamate dosage increased by 15 mg/kg daily every wk. Maximum: 3,600 mg daily or 45 mg/kg daily.
DOSAGE ADJUSTMENT Dosage reduced by 50% in patients with renal impairment.

Mechanism of Action

May exert anticonvulsant effects by antagonizing the amino acid glycine. When glycine binds to N-methyl-D-aspartate (NMDA) receptors in the CNS, the frequency at which receptor-gated calcium ion channels open is increased—an important factor in initiating seizures. Felbamate may raise the seizure threshold by blocking NMDA receptors so glycine can’t bind to them.

Contraindications

Hepatic dysfunction; history of blood dyscrasias; hypersensitivity to felbamate, other carbamates, or their components

Interactions

carbamazepine: Decreased blood carbamazepine level and increased felbamate clearance, resulting in decreased blood felbamate level fosphenytoin,
phenytoin: Increased blood phenytoin level and increased felbamate clearance, resulting in decreased blood felbamate level methsuximide: Increased adverse effects of methsuximide oral contraceptives: Possibly decreased effectiveness of oral contraceptives phenobarbital: Decreased blood felbamate level, increased blood phenobarbital level and risk of adverse effects
valproic acid: Increased blood valproic acid level and increased risk of adverse effects

Side Efect

CNS: Abnormal gait, aggressiveness, agitation, anxiety, dizziness, drowsiness, fever, headache, insomnia, mood changes, suicidal ideation, tremor
EENT: Altered taste, diplopia, rhinitis
GI: Abdominal pain, anorexia, constipation, diarrhea, elevated liver function test results, hepatic failure, indigestion, nausea, vomiting
HEME: Aplastic anemia, leukopenia, pancytopenia, thrombocytopenia
RESP: Upper respiratory tract infection
SKIN: Photosensitivity, purpura, rash
Other: Anaphylaxis, lymphadenopathy, weight loss

Cautions

Check liver function test results before starting felbamate, and expect to check results every 1 to 2 weeks during treatment. Notify prescriber immediately and expect to stop drug if results are abnormal.

Plan to taper dosage by one-third every 4 to 5 days as prescribed. If patient receives adequate amounts of other anticonvulsant , felbamate may be felbamate 425 E F stopped without tapering, if needed.
WARNING Assess for signs of aplastic anemia and bone marrow depression. Signs may not appear until several months after therapy begins. Expect to stop felbamate if bone marrow depression develops.

If patient receives adjunctive therapy, expect

Side Efect

to resolve as other anticonvulsant dosages decrease.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

PATIENT SAFTY

Direct patient to shake suspension before using and to use a calibrated spoon or container to measure each dose.

Instruct patient to store oral suspension and tablets at room temperature.

Because drug may cause photosensitivity, urge patient to protect skin from sun and to avoid sunlamps and tanning booths.

Explain that dizziness and drowsiness may occur. Advise her to avoid hazardous activities until drug’s CNS effects are known.

Warn patient not to stop drug abruptly.

Advise patient to return for ordered liver function tests and to report yellow skin or eyes and dark urine to prescriber.

Instruct patient to tell prescriber if she experiences bleeding, infection, or fatigue.

Advise patient to carry medical identification that indicates condition and therapy.

Because felbamate decreases oral contraceptive effectiveness, discuss alternate contraceptive methods.

Urge caregivers to watch patient closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes, and to report any concerns immediately.

Encourage female patient who becomes pregnant while taking felbamate to enroll in the North American antiepileptic drug pregnancy registry by calling 1-888-2332334. Explain that this registry is collecting information about the safety of antiepileptic during pregnancy.

Category

Chemical class: Dihydropyridine derivative
Therapeutic class: Antihypertensive

Pregnancy category: C

Indications

To manage essential hypertension alone or with other antihypertensives
Adults.Initial: 5 mg daily. Dosage adjusted every 2 wk to 2.5 to 10 mg daily based on patient response.
DOSAGE ADJUSTMENT Initial or maintenance dosage reduced, if needed, in patients who are over age 65 or have impaired hepatic function. Route Onset Peak Duration P.O. 2–5 hr Unknown 16–24 hr

Mechanism of Action

May slow the movement of extracellular calcium into myocardial and vascular smooth-muscle cells by deforming calcium channels in cell membranes, inhibiting ioncontrolled gating mechanisms, and interfering with calcium release from the sarcoplasmic reticulum. The effect of these actions is a decrease in intracellular calcium ions, which inhibits contraction of smooth-muscle cells and dilates coronary and systemic arteries. As with other calcium channel blockers, felodipine’s actions result in increased oxygen to the myocardium and reduced peripheral resistance, blood pressure, and afterload.

Contraindications

Hypersensitivity to felodipine or its components

Interactions

anesthetics (hydrocarbon inhalation): Possibly hypotension antihypertensives, prazocin: Increased risk of hypotension
beta blockers: Increased adverse effects of beta blockers
cimetidine: Increased felodipine bioavailability digoxin: Transiently increased blood digoxin level and risk of digitalis toxicity estrogens: Possibly increased fluid retention and decreased felodipine effects lithium: Increased risk of neurotoxicity NSAIDs, sympathomimetics: Possibly felodipine 426 decreased therapeutic effect of felodipine procainamide,
quinidine: Increased risk of prolonged Q-T interval tacrolimus: Possibly increased blood tacrolimus level and risk of adverse effects grapefruit juice: Doubled felodipine bioavailability

Side Efect

CNS: Asthenia, dizziness, drowsiness, fatigue, headache, paresthesia, syncope, weakness
CV: Chest pain, hypotension, palpitations, peripheral edema, tachycardia
EENT: Gingival hyperplasia, pharyngitis, rhinitis
GI: Abdominal cramps, constipation, diarrhea, indigestion, nausea
HEME: Agranulocytosis
MS: Back pain
RESP: Cough
SKIN: Flushing, rash

Cautions

Use felodipine cautiously in patients with heart failure or reduced ventricular function.

Monitor blood pressure during dosage titration and throughout felodipine therapy, especially in elderly patients.

Felodipine bioavailability increases up to twofold when taken with grapefruit juice.
WARNING Felodipine may cause severe hypotension with syncope, which may lead to reflex tachycardia. This can precipitate angina in patients with coronary artery disease or a history of angina.

Watch for signs of overdose, such as excessive peripheral vasodilation, marked hypotension and, possibly, bradycardia. If they appear, place patient in supine position with legs elevated and give I.V. fluids, as ordered. Expect to give I.V. atropine for bradycardia.

PATIENT SAFTY

Instruct patient to swallow tablets whole and not to crush or chew them.

Caution patient not to alter her intake of grapefruit juice during therapy.

Advise patient to store felodipine at room temperature and to protect it from light.

Instruct patient to monitor her pulse rate and blood pressure.

Teach patient how to minimize gingival hyperplasia.

Advise patient to notify prescriber immediately if she has palpitations, pronounced dizziness, or swelling of hands or feet.

Category

Chemical class: Aryloxisobutyric acid derivative
Therapeutic class: Antihyperlipidemic

Pregnancy category: C

Indications

To treat primary hypercholesterolemia or mixed hyperlipidemia
Adults.200 mg daily.
Adults. 145 mg daily. To treat hypertriglyceridemia (Fredrickson types IV and V hyperlipidemia)
Adults. Initial: 67 mg daily with food, increased as needed every 4 to 8 wk. Maximum: 201 mg daily with meals.
Adults. 48 to 145 mg daily, increased as needed at 4to 8-wk intervals. Maximum: 145 mg daily.
DOSAGE ADJUSTMENT For patients with mild to moderate renal impairment, initial dosage limited to 48 mg daily (tablets) or 67 mg daily (capsules), with dosage increase only after drug’s therapeutic and renal effects are known. For elderly patients, dosage limited to 48 mg daily (tablets) or 67 mg daily (capsules). As adjunct to diet to treat severe hypertriglyceridemia DELAYED-RELEASE
Adults. Initial: 45 mg once daily, increased, as needed every 4to 8-wk intervals. Maximum: 135 mg daily. As adjunct to diet to treat primary hyperlipidemia or mixed dyslipidemia; as adjunct to diet and a HMG-CoA fenofibrate 427 E F reducatse inhibitor to treat mixed dyslipidemia DELAYED-RELEASE
Adults.135 mg daily.
DOSAGE ADJUSTMENT For patients with mild to moderate renal impairment or elderly patients, initial dosage limited to 45 mg once daily, with increase only after drug’s therapeutic and renal effects are known. Route Onset Peak Duration P.O. 6–8 wk Unknown Unknown

Mechanism of Action

May increase the lipolysis of triglyceriderich lipoproteins and decrease the synthesis of fatty acids and triglycerides by enhancing the activation of lipoprotein lipase and acyl-coenzyme A synthetase. Fenofibrate also may:

increase hepatic elimination of cholesterol as bile salts

promote the catabolism of larger, less dense LDLs with a high-binding affinity for cellular LDL receptors.

Contraindications

Breast-feeding; gallbladder disease; hypersensitivity to fenofibrate, fenofibric acid, choline fenofibrate, or their components; hepatic or severe renal impairment

Interactions

bile acid sequestrants: Decreased fenofibrate absorption cyclosporine: Increased risk of nephrotoxicity HMG-CoA reductase inhibitors (atorvastatin, cerivastatin, fluvastatin, lovastatin, pravastatin, simvastatin): Increased risk of myopathy, rhabdomyolysis, and acute renal failure oral anticoagulants: Risk of bleeding all : Increased fenofibrate bioavailability when given in capsule form

Side Efect

CNS: Asthenia, fatigue, headache
CV: Deep vein thrombosis
EENT: Rhinitis
GI: Abdominal pain, cholelithiasis, cirrhosis, constipation, diarrhea, elevated liver function test results, hepatitis, nausea, pancreatitis
GU: Increased serum creatinine level, renal failure
HEME: Agranulocytosis, anemia, decreased hematocrit and hemoglobin levels, thrombocytopenia
MS: Arthralgia, back pain, muscle spasms, myopathy. myositis, rhabdomyolysis
RESP: Pulmonary embolus
SKIN: Rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Flulike symptoms

Cautions

As ordered, stop that increase serum triglycerides, such as beta blockers, estrogens, and thiazides, and obtain baseline lipid levels before starting fenofibrate.

Give capsule form with a full glass of water with meals.

Administer drug 1 hour before or 4 hours after bile acid sequestrants.

Monitor results of liver and renal function tests. If liver enzyme levels rise to more than three times the upper limit of normal and persist, or if the patient develops gallstones, expect to stop drug.

Monitor serum triglyceride and cholesterol levels at 4to 8-week intervals. If levels don’t decrease after 2 months at maximum dosage, expect to stop therapy.
WARNING Monitor patient closely for acute hypersensitivity reactions, including severe rash, and notify prescriber if they occur. Patient may need inpatient corticosteroids.

Assess blood counts periodically, as ordered, during first 12 months of therapy to detect adverse hematologic effects.

Watch closely for evidence of deep vein thrombosis (pain, swelling, redness in extremity) or pulmonary embolus (sudden onset of anxiety, shortness of breath, restlessness) because risk is higher in patients taking fenofibrate. Notify prescriber immediately, and start emergency treatment, as prescribed.

PATIENT SAFTY

Stress that drug will be effective only if patient carefully follows prescriber’s instructions about diet and exercise.

Instruct patient to take capsule form with a full glass of water and with food.

Instruct patient prescribed tablet form to store the tablets in their original, desiccant-containing bottle and to avoid taking any chipped or broken tablets. fenofibrate 428

Advise patient to have laboratory tests, as directed, to determine drug’s effectiveness. They typically include liver function tests after 3 to 6 months, hematocrit and hemoglobin levels, and WBC counts periodically during first year.

Urge patient to notify prescriber immediately about chills, fever, or sore throat. Also urge her to tell prescriber about unexplained muscle pain, tenderness, or weakness, especially if accompanied by fatigue or fever.

Tell patient to seek emergency treatment if he develops pain, swelling, and redness in his limb or sudden shortness of breath, anxiety, and restlessness.

Category

Chemical class: Dopamine agonist
Therapeutic class: Antihypertensive

Pregnancy category: B

Indications

To treat severe hypertension when rapid, but quickly reversible, emergency reduction of blood pressure is clinically indicated, including malignant hypertension with deteriorating end-organ function
IV:
Adults. Initial: 0.025 to 0.3 mcg/kg/min, individualized according to patient weight and desired effect. Usual: 0.01 to 1.6 mcg/ kg/min. Maximum: 1.6 mcg/kg/min for up to 48 hr. Route Onset Peak Duration I.V. Rapid Unknown Unknown

Mechanism of Action

Stimulates dopamine-1 postsynaptic receptors, which mediate renal and mesenteric vasodilation.Vasodilation lowers blood pressure and total peripheral resis-tance while increasing renal blood flow.

Contraindications

Hypersensitivity to fenoldopam or its components

Interactions

antihypertensives: Additive hypotensive effect
beta blockers: Increased risk of hypotension dopamine antagonists, metoclopramide: Possibly decreased effects of fenoldopam

Side Efect

CNS: Anxiety, headache, light-headedness
CV: Hypotension, STand T-wave changes, tachycardia
EENT: Increased intraocular pressure
GI: Abdominal pain, nausea
SKIN: Diaphoresis, flushing
Other: Hypokalemia, injection site pain

Cautions

Reconstitute by adding 40 mg fenoldopam (4 ml of concentrate) to 1,000 ml normal saline solution or D5W, or 20 mg fenoldopam (2 ml of concentrate) to 500 ml normal saline solution or D5W, or 10 mg fenoldopam (1 ml of concentrate) to 250 ml normal saline solution or D5W to produce a final fenoldopam concentration of 40 mcg/ml.

Infuse through a mechanical infusion pump for proper control of infusion rate.

Expect to titrate fenoldopam dosage in increments of 0.05 to 0.1 mcg/kg/min, as prescribed.

Expect to monitor heart rate and blood pressure every 15 minutes during therapy because most effect on blood pressure occurs within 15 minutes of any dosage change.

Be aware that patient may be started on oral antihypertensive therapy, as prescribed, any time after blood pressure is stable during fenoldopam infusion.

Discard any reconstituted solution not used within 24 hours.
WARNING Assess patient for signs of increased myocardial oxygen demand, especially if patient has heart failure or a history of angina, because fenoldopam may produce a rapid decline in blood pressure, resulting in symptomatic hypotension and a dose-dependent increase in heart rate.

Monitor serum potassium level because fenoldopam decreases serum potassium concentrations, which may result in hypokalemia, exacerbate arrhythmias, or fenoldopam mesylate 429 E F precipitate conduction abnormalities, especially in patients with cardiac disease.

Monitor patients with glaucoma or increased intraocular pressure for changes in vision because drug may cause a dosedependent increase in intraocular pressure.

Be alert for possible allergicor anaphylactic-type reaction to sodium metabisulfite, a component of fenoldopam injection, especially in patients with asthma.

PATIENT SAFTY

Inform patient that she’ll be switched to an oral antihypertensive once her blood pressure is controlled.

Instruct patient to expect frequent monitoring of vital signs.

Category

Chemical class: Propionic acid derivative
Therapeutic class: Analgesic, antiinflammatory, antirheumatic

Pregnancy category: Not rated

Indications

To manage mild to moderate pain ,
Adults. 200 mg every 4 to 6 hr, as needed. To relieve pain, stiffness, and swelling from rheumatoid arthritis or osteoarthritis ,
Adults. 300 mg or 400 mg to 600 mg t.i.d. or q.i.d. Maximum: 3,200 mg daily. Route Onset Peak Duration P.O. 15–30 Unknown 4–6 hr min*

Mechanism of Action

Blocks the activity of cyclooxygenase, the enzyme needed for prostaglandin synthesis. Prostaglandins, important mediators of the inflammatory response, cause local vasodilation with swelling and pain. When cyclooxygenase is blocked and prostaglandins inhibited, inflammatory symptoms subside. Prostaglandin inhibition also relieves pain because prostaglandins play a role in pain transmission from the periphery to the spinal cord.

Contraindications

Angioedema, asthma, bronchospasm, nasal polyps, rhinitis, or urticaria induced by aspirin, iodides, or NSAIDs; hypersensitivity to fenoprofen or its components; renal impairment; severe hepatic impairment

Interactions

acetaminophen: Increased risk of renal impairment with concurrent long-term use antacids: Decreased fenoprofen effectiveness anticoagulants, cefamandole, cefoperazone, cefotetan, heparin, plicamycin, thrombolytics,
valproic acid: Increased risk of bleeding antineoplastics: Increased adverse hematologic effects cyclosporine: Increased risk of nephrotoxicity diuretics, triamterene: Decreased effectiveness of these glucocorticoids, NSAIDs, potassium supplements: Increased adverse GI effects insulin, oral antidiabetic : Increased risk of hypoglycemia lithium: Increased risk of lithium toxicity methotrexate: Increased risk of methotrexate toxicity phenobarbital: Possibly decreased elimination half-life of fenoprofen salicylates: Increased risk of GI bleeding alcohol use, smoking: Increased risk of GI bleeding

Side Efect

CNS: Agitation, confusion, dizziness, drowsiness, headache, seizures, sleep disturbance, stroke, tremor, weakness
CV: Hypertension, MI, palpitations, peripheral edema, tachycardia, vasodilation
EENT: Blurred vision, dry or sore mouth, hearing loss, tinnitus
GI: Abdominal cramps, distention, and pain; anorexia; constipation; diarrhea; diverticulitis; dysphagia; esophagitis; flatulence; gastritis; gastroenteritis; gastroefenoprofen calcium 430 * For analgesia; 2 days for antirheumatic effects. For analgesia; 2 to 3 wk for antirheumatic effects. For analgesia; unknown for antirheumatic effects. sophageal reflux disease; GI bleeding or ulceration; hemorrhoids; hepatitis; hiatal hernia; indigestion; jaundice; liver failure; melena; nausea; perforation of stomach or intestines; vomiting
GU: Acute renal failure, dysuria, interstitial nephritis
HEME: Agranulocytosis, anemia, hemolytic anemia, leukopenia, neutropenia, pancytopenia
MS: Muscle spasms and twitching, myalgia
RESP: Dyspnea
SKIN: Diaphoresis, erythema, erythema multiforme, exfoliative dermatitis, pruritus, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema

Cautions

Use fenoprofen with extreme caution in patients with a history of ulcer disease or GI bleeding because NSAIDs such as fenoprofen increase risk of GI bleeding and ulceration. Expect to use fenoprofen for the shortest time possible in these patients.

Serious GI tract ulceration, bleeding, and perforation may occur without
WARNING symptoms. Elderly patients are at greater risk. To minimize risk, give drug with food. If GI distress occurs, withhold drug and notify prescriber immediately.

Use fenoprofen cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.

Give drug with food, milk, or antacids to decrease adverse GI reactions.

Patients with rheumatoid arthritis may need higher doses than those with osteoarthritis to control their symptoms.
WARNING If patient receives long-term therapy, watch for signs of toxicity, such as agitation; blurred vision; coma; confusion; drowsiness; elevated BUN and serum creatinine levels; indigestion; nausea; rash; seizures; severe headache; slow, labored breathing; tinnitus; and vomiting.
WARNING Monitor patient closely for thrombotic events, including MI and stroke, because NaSAIDs increase the risk.
WARNING If patient has bone marrow suppression or is receiving antineoplastic drug therapy, monitor laboratory results (including WBC count), and watch for evidence of infection because anti-inflammatory and antipyretic actions of fenoprofen may mask signs and symptoms of infection, such as fever and pain.

Monitor patient—especially if she’s elderly or receiving long-term fenoprofen therapy—for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor patient’s liver function test results because, in rare cases, elevations may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in elderly patients, patients taking diuretics or ACE inhibitors, and patients with heart failure, impaired renal function, or hepatic dysfunction because drug may cause renal failure.

Monitor CBC for decreased hemoglobin and hematocrit because drug may worsen anemia.

Assess patient’s skin regularly for signs of rash or other hypersensitivity reaction because fenoprofen is an NSAID and may cause serious skin reactions without warning, even in patients with no history of NSAID sensitivity. At first sign of reaction, stop drug and notify prescriber.

PATIENT SAFTY

Advise patient to take fenoprofen with food, milk, or antacids to minimize GI distress. Also instruct her to take drug with a full glass of water and to stay upright for 30 minutes afterward to decrease the risk of drug lodging in the esophagus and causing irritation.

Instruct patient to swallow drug whole and not to crush, break, chew, or open capsules.

Caution patient to avoid alcohol, aspirin, and other NSAIDs, unless prescribed, while taking fenoprofen.

If patient takes an anticoagulant, urge her to immediately report bleeding, including bloody or tarry stools and bloody vomitus.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Explain that NSAIDs may increase the risk of serious adverse cardiovascular reactions; urge patient to seek immediate fenoprofen calcium 431 E F medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.

Explain that fenoprofen also may increase the risk of serious adverse GI reactions; stress the need to seek immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.

Alert patient to the possibility of rare but serious skin reactions. Urge her to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity. fentanyl citrate Actiq,Onsolis,Sublimaze fentanyl transdermal system Duragesic fentanyl

Category

Therapeutic class: Analgesic, anesthesia adjunct

Pregnancy category: C

Controlled substance schedule: II

Indications

To provide surgical premedication
I.M.INJECTION
Adults. 0.05 to 0.1 mg 30 to 60 min before surgery. As adjunct to regional anesthesia I.V.OR
I.M.INJECTION
Adults. 0.05 to 0.1 mg I.M. or slow I.V. over 1 to 2 min. To manage postoperative pain in postanesthesia care unit
I.M.INJECTION
Adults. 0.05 to 0.1 mg. Repeated in 1 to 2 hr, if needed. To manage acute postoperative pain in hospitalized patients requiring opioid analgesia IONTOPHORETIC TRANSDERMAL
Adults.40 mg on-demand, released over 10 min. Maximum: Six 40-mcg doses/hour and eighty 40-mcg doses/24 hours for maximum of 72 hours. To treat breakthrough pain in cancer patients who are receiving opioid therapy and have developed tolerance to it TRANSMUCOSAL LOZENGE(ACTIQ)
Adults. Initial: 200 mcg placed between cheek and gum for up to 15 min followed by second dose 15 min after first dose ends, if needed. Dosage increased according to patient’s needs. TRANSMUCOSAL SOLUBLE FILM(ONSOLIS)
Adults. Initial: 200-mcg film sheet placed against inside of cheek per episode. Increased, as needed, by 200 mcg in each subsequent episode, with doses at least 2 hours apart. Maximum: Four 200-mcg film sheets or one 1,200-mcg film sheet four times daily. To relieve persistent moderate to severe chronic pain that doesn’t respond to less potent and requires around-theclock opioid administration for an extended time TRANSDERMAL SYSTEM Adults and children age 2 and over. Initial: One 25-mcg/hr patch, replaced every 72 hr (or 48 hr, if needed). Dosage increased by 12.5 mcg/hr, as needed, after first 72 hr and then every 6 days. For more than 100 mcg/ hr, more than one patch is used.
DOSAGE ADJUSTMENT For elderly, cachectic, or debilitated patients, initial dosage should not exceed 25 mcg/hr unless patient is already receiving more than 135 mg of oral morphine daily or an equivalent dose of another opioid. For patients receiving longterm opioid therapy, dosage adjusted based on previous day’s drug requirement. For cancer patients who need more than 800 mcg/day for breakthrough pain, dosage altered or another long-acting opioid given, as prescribed.

Mechanism of Action

Binds to opioid receptor sites in the CNS, altering perception of and emotional response to pain by inhibiting ascending pain pathways. Fentanyl may alter neurofentanyl 432 transmitter release from afferent nerves responsive to painful stimuli, and it causes respiratory depression by acting directly on respiratory centers in the brain stem. Route Onset Peak Duration I.V. 1–2 min 3–5 min 30–60 min I.M. 7–15 min 20–30 min 1–2 hr Trans12–24 hr Unknown Over 72 hr dermal

Contraindications

I.V. or I.M. form: Under age 2, asthma, myasthenia gravis, opioid hypersensitivity or intolerance Transmucosal form: Acute or chronic pain, including postoperative pain Transdermal form: Acute or postoperative pain, under age 12 (under age 18 if weight is less than 50 kg [110 lb]), dosage that exceeds 25 mcg/hr at the start of therapy, hypersensitivity to fentanyl (or alfentanil, sufentanil, or adhesives), intermittent pain, treatment of mild to moderate pain responsive to nonopioid All for
MS: Hypersensitivity to fentanyl (or alfentanil, sufentanil, or adhesives) or its components, intermittent pain, opioid nontolerance, significant respiratory depression, treatment of mild to moderate pain responsive to nonopioid , upper airway obstruction

Interactions

amiodarone, amprenavir, aprepitant, clarithromycin, diltiazem, erythromycin, fluconazole, fosamprenavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, troleandomycin, verapamil: Possibly increased opioid effect, leading to increased or prolonged adverse effects, including severe respiratory depression anticholinergics, antidiarrheals (such as loperamide and paregoric): Increased risk of severe constipation antihypertensives, diuretics: Possibly potentiated hypotension benzodiazepines: Possibly reduced fentanyl dose required for anesthesia induction buprenorphine: Possibly decreased therapeutic effects of buprenorphine
CNS depressants: Possibly increased CNS and respiratory depression and hypotension cytochrome P-450 inducers (such as rifampin, carbamazepine, and phenytoin): Possibly induced metabolism and increased clearance of fentanyl hydroxyzine: Possibly increased analgesic effect of fentanyl and increased CNS depression and hypotension
MAO inhibitors: Possibly unpredictable or fatal effects if taken within 14 days metoclopramide: Possibly antagonized effect of metoclopramide on gastric motility nalbuphine, pentazocine: Possibly antagonized analgesic, respiratory depressant, and CNS depressant effects of fentanyl; possibly additive hypotensive and CNS and respiratory depressant effects of both naloxone: Antagonized analgesic, hypotensive, CNS, and respiratory depressant effects of fentanyl
naltrexone: Possibly blocked therapeutic effects of fentanyl neuromuscular blockers: Possibly prevention or reversal of muscle rigidity by fentanyl grapefruit juice: Increased blood fentanyl level
alcohol use: Increased CNS and respiratory depression and hypotension

Side Efect

CNS: Agitation, amnesia, anxiety, asthenia, ataxia, confusion, delusions, depression, dizziness, drowsiness, euphoria, fever, hallucinations, headache, lack of coordination, light-headedness, nervousness, paranoia, sedation, seizures, sleep disturbance, slurred speech, syncope, tremor, weakness, yawning
CV: Asystole, bradycardia, chest pain, edema, hypotension, orthostatic hypotension, tachycardia
EENT: Blurred vision, dental caries, dry mouth, gum line erosion, laryngospasm, rhinitis, sneezing, tooth loss
GI: Anorexia, constipation, ileus, indigestion, nausea, vomiting
GU: Anorgasmia, decreased libido, ejaculatory difficulty, urinary hesitancy, urine retention
RESP:Apnea, depressed cough reflex, dyspnea, hypoventilation, respiratory depression
SKIN: Diaphoresis, exfoliative dermatitis, localized skin redness and swelling (with transdermal form), pruritus, rash
Other: Anaphylaxis, drug tolerance, physifentanyl 433 E F cal or psychological dependence with longterm use, weight loss

Cautions

WARNING Fentanyl transdermal system should be used only in patients already receiving opioid therapy and with demonstrated opioid tolerance (taking for a week or longer at least 60 mg of morphine daily, 30 mg of oral oxycodone daily, 8 mg of oral hydromorphone daily, or an equianalgesic dose of another opioid), and require at least a fentanyl dosage of 25 mcg per hour to manage their pain.

Use caution when titrating fentanyl dosage in elderly patients, especially using intravenous route, because these patients are more sensitive to the drug’s effects.

Use cautiously in patients at risk for opioid abuse, such as those with mental illness or personal or family history of substance abuse. Monitor patient throughout therapy for fentanyl abuse or addiction.

To reduce skin irritation, spray the allergy inhaler triamcinolone on the patient’s skin, as prescribed, before applying a fentanyl patch.

Expect the blood fentanyl level to be prolonged if patient chews or swallows the transmucosal form because drug is absorbed slowly from GI tract.
WARNING Never apply a transdermal patch if seal has been broken or patch has been cut, damaged, or changed because excessive exposure could occur, resulting in possibly fatal fentanyl overdose.

Be aware that 100 mcg of fentanyl is equivalent in potency to 10 mg of morphine.

To achieve optimum pain control with the lowest possible fentanyl dose, also plan to give a nonopioid analgesic, such as acetaminophen, as prescribed.
WARNING Monitor patient’s respiratory status closely, especially during the first 24 to 72 hours after therapy starts or dosage increases, because severe hypoventilation may occur without
WARNING at any time during therapy.

To prevent withdrawal symptoms after long-term use, expect to taper drug dosage gradually, as prescribed.

Assess patient for withdrawal symptoms after dosage reduction or conversion to another opioid analgesic.

For patient with bradycardia, implement cardiac monitoring, as ordered, and assess heart rate and rhythm frequently during fentanyl therapy because drug may further slow heart rate.
WARNING Expect respiratory depressant effects to last longer than analgesic effects. Also be prepared for residual drug to potentiate effects of subsequent doses. Residual drug can be detected for at least 6 hours after I.V. dose and 17 hours after other forms. Monitor patient closely for at least 24 hours after therapy ends.
WARNING Assess patient for evidence of overdose, such as cardiopulmonary arrest, hypoventilation, pupil constriction, respiratory and CNS depression, seizures, and shock. Give naloxone (possibly in repeated doses), as prescribed. Be prepared to assist with endotracheal intubation and mechanical ventilation and to provide fluids.

Monitor blood glucose level of diabetic patient receiving transdermal fentanyl because each unit contains about 2 g of sugar.
WARNING Do not substitute Actiq or Onsolis for any other fentanyl product and do not substitute for each other. Do not convert dosage to or from other products on a mcg-per-mcg basis because doing so may result in a fatal overdose.

PATIENT SAFTY

Instruct patient to avoid alcohol and other CNS depressants during fentanyl therapy unless prescribed.

Advise patient not to stop taking drug unless directed by prescriber because withdrawal symptoms may occur. Warn against increasing dose or frequency without consulting prescriber because drug can cause dependency.

For transdermal form, instruct patient to choose a site with intact (not irritated or irradiated) skin on a flat surface, such as the chest, back, flank, or upper arm, and, if appropriate, to clip, not shave, hair from the site and clean it with water (no soaps, lotions, oils, or alcohol). After site preparation, instruct patient to press patch firmly in place with palm for 30 seconds, making sure edges are sealed. If patch loosens, tell her to tape edges down but not cover the entire patch. If more than one patch is needed, the edges shouldn’t fentanyl 434 touch or overlap. Instruct patient to remove patch after 72 hours, fold it in half with adhesive sides together, and flush it down the toilet. Remind her not to reuse a site for at least 3 days.

Warn patient never to apply transdermal patch if seal has been broken or the patch has been cut, damaged, or changed in any way because drug may be released too rapidly. Also warn patient not to expose the application site and surrounding area to direct external heat sources, such as heating pads or electric blankets, heat or tanning lamps, saunas, hot tubs, and heated water beds, while wearing the patch. She should also avoid hot baths or sunbathing because increased body temperature may increase fentanyl release, resulting in a possible overdose. If she develops a fever or becomes overheated from strenuous exercise while wearing a patch, she should contact the prescriber immediately.

For iontophoretic transdermal form, instruct patient to press button twice firmly within 3 seconds to release a dose. An audible tone will sound when a dose is activated, and a red light will stay on throughout the 10-minute administration. Explain that no more than six doses can be given per hour and no more than 80 doses per 24 hours. Tell the patient that the patch may be replaced once 80 doses are released or 24 hours pass, but that 72 hours is the maximum time the drug can be delivered in this way.

For Actiq transmucosal form, instruct patient to open the package just before use and to save plastic cap for discarding the unused part of the lozenge. Tell her to place lozenge between her cheek and gum and to suck, not chew, it for 15 minutes. Show her how to move lozenge from one side of her mouth to the other using the handle provided separately.

For Onsolis transmucosal form, instruct patient to wet inside of cheek with tongue or rinse his mouth with water. Tell him to open package just before use and place entire film sheet on the tip of a dry finger, pink side facing up. Then he should carefully place pink side of film against inside of cheek and press and hold it in place for 5 seconds. Tell him not to drink anything for 5 minutes or eat for 30 minutes. Warn patient not to cut or tear film before use. If he uses multiple film sheets, tell him to place them in separately along sheek wall, not on top of each other.

Onsolis dosage increases must occur only in 200-mcg increments, must be done only in later pain episodes, and must be separated by at least 2 hours from previous dose. If pain isn’t relieved within 30 minutes, tell him not to use another dose but to use a rescue drug instead. If dosage increase is needed and continues to be needed, tell patient to contact prescriber for new dosage strength because each episode should be treated with one film sheet of appropriate strength.

For transmucosal form, urge patient to see a dentist regularly, to brush teeth and floss after each meal, and to avoid frequent consumption of products high in sugar because of increased risk of dental caries.

For transmucosal form, inform diabetic patient that each unit contains 2 g of sugar. Instruct her to monitor her blood glucose levels closely.

Remind patient to keep used and unused dosage units out of reach of children and to dispose of drug properly. For buccal tablets, patient should flush leftover drug down the toilet when no longer needed.

Caution patient that accidentally exposing others to transdermal fentanyl could cause serious

Side Efect

. If accidental exposure occurs, the person should remove the patch, wash the area well with water, and seek medical attention.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Tell patient to increase fiber and fluid intake, unless contraindicated, because drug may cause severe constipation. If it persists or becomes severe, urge patient to notify prescriber.

Category

Chemical class: Trace element, mineral
Therapeutic class: Antianemic, nutritional supplement

Pregnancy category: Not rated

Indications

To prevent iron deficiency based on U.S. and Canadian recommended daily allowances CAPLETS,,CHEWABLE,DRIED ,DRIED ,DRIED ,DRIED,ELIXIR,ENTERIC-COATED ,,,ORAL SOLUTION,ORAL SUSPENSION,SYRUP, Adult men and children age 11 and over. 10 mg (8 to 10 mg Canadian) elemental iron daily. Adult women and children age 11 and over.10 to 15 mg (8 to 13 mg Canadian) elemental iron daily. Pregnant women.30 mg (17 to 22 mg Canadian) elemental iron daily. Breast-feeding women.15 mg (8 to 13 mg Canadian) elemental iron daily. Children ages 7 to 10. 10 mg (8 to 10 mg Canadian) elemental iron daily. Children ages 4 to 6. 10 mg (8 mg Canadian) elemental iron daily. Children from birth to age 3. 6 to 10 mg (0.3 to 6 mg Canadian) elemental iron daily. To replace iron in deficiency states CAPLETS,,CHEWABLE,DRIED ,DRIED ,DRIED ,DRIED,ELIXIR,ENTERIC-COATED ,,,ORAL SOLUTION,ORAL SUSPENSION,SYRUP, Adults and adolescents. 100 to 200 mg elemental iron t.i.d. for 4 to 6 mo. Children ages 2 to 12 weighing 30 to 50 kg (66 to 110 lb). 50 to 100 mg elemental iron daily in divided doses t.i.d. or q.i.d. for 4 to 6 mo. Children ages 6 months to 2 years.Up to 6 mg/kg elemental iron daily in divided doses t.i.d. or q.i.d. for 4 to 6 mo. Infants under age 6 months.10 to 25 mg elemental iron daily in divided doses t.i.d. or q.i.d. for 4 to 6 mo. To provide iron supplementation during pregnancy CAPLETS,,CHEWABLE,DRIED ,DRIED ,DRIED ,DRIED,ELIXIR,ENTERIC-COATED ferrous salts 436 ,,,ORAL SOLUTION,ORAL SUSPENSION,SYRUP, Pregnant women. 15 to 30 mg elemental iron daily during second and third trimesters.
DOSAGE ADJUSTMENT Dosage increased if needed for elderly patients, who may not absorb iron as easily as younger adults do.

Mechanism of Action

Acts to normalize RBC production by binding with hemoglobin or by being oxidized and stored as hemosiderin or aggregated ferritin in reticuloendothelial cells of the liver, spleen, and bone marrow. Iron is an essential component of hemoglobin, myoglobin, and several enzymes, including cytochromes, catalase, and peroxidase. Iron is needed for catecholamine metabolism and normal neutrophil function.

Contraindications

Hemochromatosis, hemolytic anemias, hemosiderosis, hypersensitivity to iron salts or their components, other anemic conditions unless accompanied by iron deficiency

Interactions

acetohydroxamic acid: Reduced absorption of both antacids, calcium supplements: Decreased iron absorption and effectiveness ascorbic acid (with doses of 200 mg or more): Increased iron absorption cholestyramine,
cimetidine: Decreased iron absorption ciprofloxacin, enoxacin, etidronate, lomefloxacin, norfloxacin, ofloxacin, oral tetracyclines: Decreased effectiveness of these dimercaprol: Possibly combination with iron in body to form a harmful chemical levodopa: Possibly chelation with iron, decreasing levodopa absorption and blood level levothyroxine: Decreased levothyroxine effectiveness and, possibly, hypothyroidism methyldopa: Decreased methyldopa absorption and efficacy penicillamine: Decreased penicillamine absorption because penicillamine chelates heavy metals vitamin E: Decreased vitamin E absorption coffee; eggs; that contain bicarbonates, carbonates, oxalates, or phosphates; milk and milk products; tea that contains tannic acid; whole-grain breads and cereals and other high-fiber : Decreased iron absorption and effectiveness alcohol abuse (acute or chronic): Increased serum iron level

Side Efect

CNS: Dizziness, fever, headache, paresthesia, syncope
CV: Chest pain, tachycardia
EENT: Metallic taste, tooth discoloration
GI: Abdominal cramps, constipation, epigastric pain, nausea, stool discoloration, vomiting
HEME: Hemochromatosis, hemolysis, hemosiderosis
RESP: Dyspnea
SKIN: Diaphoresis, flushing, rash, urticaria

Cautions

Give iron tablets and capsules with a full glass of water or juice. Don’t crush enteric-coated tablets or open capsules.

Because iron solutions may stain teeth, dilute and administer with a straw or place drops in back of patient’s throat. Mix the elixir form in water. Fer-In-Sol Drops or Syrup may be mixed with water or juice.

To maximize absorption, give iron salts 1 hour before or 2 hours after meals. If GI irritation occurs, give with or just after meals.

Protect liquid form from freezing.

Be aware that at usual dosages, serum hemoglobin level usually normalizes in about 2 months unless blood loss continues. Treatment lasts for 3 to 6 months to help replenish iron stores.
WARNING Monitor patient for signs of iron overdose, which may include abdominal pain, diarrhea (possibly bloody), nausea, severe vomiting, and sharp abdominal cramps. In case of iron toxicity or accidental iron overdose (a leading cause of fatal poisoning in children under age 6), give deferoxamine, as prescribed.As few as 3 adult iron tablets can cause serious poisoning in young children.

Don’t give antacids, coffee, tea, dairy products, eggs, or whole-grain cereals or breads within 1 hour before or 2 hours after iron.

Remember that unabsorbed iron turns ferrous salts 437 E F stool green or black and can mask blood in stool. Check stool for occult blood, as ordered.

PATIENT SAFTY

Instruct patient not to chew any solid form of iron except for chewable tablets.

Inform patient that iron deficiency may cause decreased stamina, learning problems, shortness of breath, and tiredness.

To improve iron absorption, urge patient to eat lean red meat, chicken, turkey, and fish as well as rich in vitamin C (such as citrus fruits and fresh vegetables).

Urge patient to avoid that impair iron absorption, including dairy products, eggs, spinach, and high-fiber , such as whole-grain breads and cereals and bran. Also advise her to avoid drinking coffee or tea within 1 hour of iron intake.

Caution patient not to take antacids or calcium supplements within 1 hour before and 2 hours after taking iron supplement.

Inform patient that stool should become dark green or black during therapy. Advise her to notify prescriber if it doesn’t.

To minimize tooth stains from liquid iron, instruct patient to mix dose with water, fruit juice, or tomato juice and to drink it with a straw. If patient must take liquid iron by dropper, direct her to place drops well back on the tongue and to follow with water or juice. Tell her that iron stains can be removed by brushing with baking soda (sodium bicarbonate) or medicinal peroxide (hydrogen peroxide 3%).

Advise patient to consult prescriber before taking large amounts of iron for longer than 6 months.

Warn patient about high risk of accidental poisoning, and urge her to keep iron preparations out of the reach of children.

Category

Chemical class: Muscarinic receptor antagonist
Therapeutic class: Antispasmodic

Pregnancy category: C

Indications

To treat overactive bladder with symptoms of urinary incontinence, urgency, and frequency
Adults.Initial: 4 mg daily, increased to 8 mg, as needed. Maximum: 8 mg daily.
DOSAGE ADJUSTMENT For patients with severe renal insufficiency or who are taking potent CYP3A4 inhibitors (such as clarithromycin, itraconazole, and ketoconazole), dosage shouldn’t exceed 4 mg daily. Route Onset Peak Duration P.O. Unknown 5 hr Unknown

Mechanism of Action

Exerts antimuscarinic (atropine-like) and potent direct antispasmodic (papaverinelike) actions on smooth muscle in the bladder. The result is increased bladder capacity and a decreased urge to void. Fesoterodine has an active metabolite that inhibits bladder contraction and decreases detrussor pressure.

Contraindications

Gastric retention, GI obstruction, hypersensitivity to fesoterodine or its components, ileus, pyloric stenosis, uncontrolled narrowangle glaucoma, urine retention

Interactions

antimuscarinic agents: Possibly increased anticholinergic effects; possibly altered absorption of oral taken concurrently potent CYP3A4 inhibitors, such as clarithromycin, itraconazole,
ketoconazole: Possibly increased serum fesoterodine level and increased risk of adverse effects caffeine: May aggravate bladder symptoms
alcohol use: Increased drowsiness

Side Efect

CNS: Drowsiness, insomnia
CV: Angina, chest pain, peripheral edema, QT-interval prolongation
EENT: Blurred vision; dry eyes, mouth, or throat
GI: Constipation, diverticulitis, dyspepsia, elevated liver enzymes, gastroenteritis, irritable bowel syndrome, nausea, upper fesoterodine fumarate 438 abdominal pain
GU: Dysuria, urine retention, UTI
MS: Back pain
RESP: Cough, upper respiratory tract infection
SKIN: Decreased sweating, rash

Cautions

Use cautiously in patients with significant bladder outlet obstruction because fesoterodine can cause urine retention.

Use cautiously in patients with myasthenia gravis, decreased GI motility, and controlled narrow-angle glaucoma because drug can make these conditions worse.

Use cautiously in patients taking other with anticholinergic effects, such as antihistamines.

PATIENT SAFTY

Instruct patient to take drug exactly as prescribed.

Tell patient to take drug with a full glass of water and not to cut, crush, or chew tablets.

Explain that drug can cause adverse effects such as constipation and urine retention. If they occur and are severe or prolonged, patient should notify prescriber.

Advise patient to avoid alcohol consumption during fesoterodine therapy.

Tell patient to avoid hazardous activities until drug’s CNS effects are known.

Caution patient to avoid strenuous exercise and excessive sun exposure because of increased risk of heatstroke.

Advise patient to limit caffeine consumption during drug therapy.

Explain that full benefits of fesoterodine therapy may take 2 to 3 months.

Inform patient that chewing sugarless gum or sucking hard candy (especially lemon drops) may help ease dry mouth.

Category

Chemical class: Granulocyte colonystimulating factor
Therapeutic class: Antineutropenic, hematopoietic stimulator

Pregnancy category: C

Indications

To prevent infection after myelosuppressive chemotherapy
IV:
Adults. 5 mcg/kg daily over 15 to 30 min. Increased, if needed, by 5 mcg/kg with each chemotherapy cycle. SUBCUTANEOUS INJECTION
Adults.5 mcg/kg daily for up to 2 wk. Increased, if needed, by 5 mcg/kg with each chemotherapy cycle. To reduce duration of neutropenia after bone marrow transplantation
IV:
Adults. 10 mcg/kg daily over 4 hr or as a continuous infusion over 24 hr. SUBCUTANEOUS INFUSION
Adults.10 mcg/kg as a continuous infusion over 24 hr. To enhance peripheral blood progenitor cell collection in autologous hematopoietic stem cell transplantation SUBCUTANEOUS INFUSION OR INJECTION
Adults. 10 mcg/kg as continuous infusion over 24 hr or a single injection, starting 4 days before first leukapheresis and continuing until last day of leukapheresis. To reduce occurrence and duration of neutropenia in congenital neutropenia SUBCUTANEOUS INJECTION
Adults. 6 mcg/kg b.i.d. To reduce the occurrence and duration of neutropenia in idiopathic or cyclic neutropenia SUBCUTANEOUS INJECTION
Adults. 5 mcg/kg daily.
DOSAGE ADJUSTMENT Dosage reduced for patients whose absolute neutrophil count remains above 10,000/mm3. Route Onset Peak Duration I.V. In 5 min Unknown Unknown

Mechanism of Action

Is pharmacologically identical to human granulocyte colony-stimulating factor, an endogenous hormone synthesized by monocytes, endothelial cells, and fibroblasts. Filgrastim induces formation of neutrophil progenitor cells by binding directly to receptors on the surface of granulocytes, filgrastim 439 E F which then divide and differentiate. It also potentiates the effects of mature neutrophils, which reduces fever and the risk of infection raised by severe neutropenia.

Incompatibilities

Don’t mix filgrastim in vial or syringe with normal saline solution because precipitate will form.

Contraindications

Hypersensitivity to filgrastim, its components, or proteins from Escherichia coli

Interactions

growth hormone: Increased bone marrow hematopoetic activity lithium: Increased neutrophil production

Side Efect

CNS: Fever, headache
CV: Transient supraventricular tachycardia
GI: Splenic rupture, splenomegaly
HEME: Leukocytosis
MS: Arthralgia; myalgia; pain in arms, legs, lower back, or pelvis
SKIN: Pruritus, rash, Sweet’s syndrome (acute febrile neutrophilic dermatosis)
Other: Anaphylaxis, injection site pain and redness

Cautions

Warm filgrastim to room temperature before injection. Discard drug if stored longer than 6 hours at room temperature or 24 hours in refrigerator.

Withdraw only one dose from a vial; don’t repuncture the vial.

Don’t shake the solution.

For continuous infusion, dilute in D5W (not normal saline solution) to produce less than 15 mcg/ml.

For subcutaneous dose larger than 1 ml, divide and give in more than one site.

After chemotherapy, give drug over 15 to 30 minutes. Don’t give within 24 hours before or after cytotoxic chemotherapy.

Be aware that needle cover on single-use prefilled syringe contains dry natural rubber and may cause sensitivity reaction. It shouldn’t be handled by allergic people.

Expect to monitor CBC, hematocrit, and platelet count two or three times weekly.

Inform prescriber and expect to stop drug if leukocytosis develops or absolute neutrophil count consistently exceeds 10,000/mm3.

Anticipate decreased response to drug if patient has received extensive radiation therapy or long-term chemotherapy.

PATIENT SAFTY

Teach patient how to prepare, administer, and store filgrastim. Caution her not to reuse needle, syringe, or vial.

Advise patient prescribed single-use prefilled syringe to notify prescriber if she has an allergy to latex because needle cover may cause sensitivity reaction.

Provide patient with puncture-resistant container for needle and syringe disposal.

Advise patient to promptly report pain in left upper quadrant of abdomen or shoulder-tip pain.

Stress the importance of returning for follow-up laboratory tests.

Category

Chemical class: 4-Azasteroid compound
Therapeutic class: Benign prostatic hyperplasia agent, hair growth stimulant

Pregnancy category: X

Indications

To treat symptomatic benign prostatic hyperplasia; to reduce the risk of symptomatic progression of benign prostatic hyperplasia when given with doxazocin
Adults. 5 mg daily. To treat male-pattern baldness
Adults.1 mg daily. Route Onset Peak Duration P.O.* Unknown 8 hr 24 hr P.O. In 3 mo Unknown Unknown

Mechanism of Action

Inhibits 5-alpha reductase, an intracellular enzyme that converts testosterone to its finasteride 440 * For benign prostatic hyperplasia. With single-dose therapy; 2 wk with multiple-dose therapy. For male-pattern baldness. metabolite (5-alpha dihydrotestosterone) in liver, prostate, and skin. The metabolite is a potent androgen partially responsible for benign prostatic hyperplasia and hair loss.

Contraindications

Age (childhood), hypersensitivity to finasteride, sex (female)

Interactions

theophylline: Decreased theophylline level

Side Efect

CNS: Asthenia, dizziness, headache
CV: Hypotension, peripheral edema
EENT: Lip swelling, rhinitis
ENDO: Gynecomastia
GI: Abdominal pain, diarrhea
GU: Decreased ejaculatory volume, decreased libido, impotence, testicular pain
MS: Back pain
RESP: Dyspnea
SKIN: Pruritus, rash, urticaria
Other: Angioedema

Cautions

Expect patient to have a digital rectal examination of the prostate before and periodically during finasteride therapy.

PATIENT SAFTY

WARNING Urge patient and female partners to use reliable contraception during therapy because semen of men who take drug can harm male fetuses. Caution women and children not to handle broken tablets.

Explain how to take drug, and urge patient to follow instructions that accompany it.

Inform patient that drug may cause decreased ejaculatory volume, decreased libido, and impotence.

Urge patient to have periodic follow-up to determine drug effectiveness.

Category

Chemical class: Flavone derivative
Therapeutic class: Urinary tract antispasmodic

Pregnancy category: B

Indications

To relieve dysuria, nocturia, suprapubic pain, urinary frequency and urgency, and urinary incontinence caused by cystitis, prostatitis, urethrocystitis, or urethrotrigonitis Adults and adolescents. 100 to 200 mg t.i.d. or q.i.d. Route Onset Peak Duration P.O. 55 min 112 min Unknown

Mechanism of Action

Relaxes muscles by cholinergic blockade and counteracts smooth-muscle spasms in the urinary tract.

Contraindications

Achalasia; GI hemorrhage; hypersensitivity to flavoxate or its components; obstruction of the duodenum, ileum, or pylorus; obstructive uropathies of the lower urinary tract

Interactions

bethanechol, metoclopramide: Possibly antagonized GI motility effects of these

Side Efect

CNS: Confusion, decreased concentration, dizziness, drowsiness, fever, headache, nervousness, vertigo
CV: Palpitations, tachycardia
EENT: Accommodation disturbances, blurred vision, dry mouth, eye pain, photophobia, worsening of glaucoma
GI: Constipation, nausea, vomiting
GU: Dysuria
HEME: Eosinophilia, leukopenia
SKIN: Decreased sweating, dermatoses, urticaria

Cautions

Monitor for eye pain if patient has glaucoma because flavoxate’s anticholinergic effects may worsen glaucoma.

PATIENT SAFTY

Caution patient about possible dry mouth and photophobia. Advise her to wear sunglasses outdoors, and suggest sugarless candy or gum, ice chips, sips of water, or saliva substitute for dry mouth.

Advise patient to avoid hazardous activiflavoxate hydrochloride 441 E F ties until CNS effects of flavoxate are known.

Caution patient not to become overheated or to take hot baths or saunas during therapy because drug reduces sweating, which can lead to dizziness, fainting, or heatstroke.

Instruct patient to notify prescriber immediately if she experiences confusion, drowsiness, dysuria, headache, high fever, hives, nausea, nervousness, palpitations, rash, tachycardia, vertigo, vision problems, vomiting, or worsening dry mouth.

Category

Chemical class: Benzamide derivative
Therapeutic class: Class IC antiarrhythmic

Pregnancy category: C

Indications

To prevent and suppress recurrent lifethreatening ventricular tachycardia
Adults.Initial: 100 mg every 12 hr (every 8 hr for some patients). Increased by 50 mg b.i.d. every 4 days, if needed, until response occurs. Maintenance: Up to 150 mg every 12 hr. Maximum: 400 mg daily.
DOSAGE ADJUSTMENT Initial dose reduced to 100 mg daily or 50 mg every 12 hr for patients with creatinine clearance less than 35 ml/min/1.73 m2. To prevent paroxysmal atrial fibrillation or flutter or paroxysmal supraventricular tachycardia
Adults. Initial: 50 mg every 12 hr (every 8 hr for some patients). Increased by 50 mg b.i.d. every 4 days, if needed, until response occurs. Maintenance: Up to 150 mg every 12 hr. Maximum: 300 mg daily.

Mechanism of Action

Achieves antiarrhythmic effect by inhibiting fast sodium channels of myocardial cell membranes, which increase myocardial recovery after repolarization, and by depressing the upstroke of the action potential. Flecainide also produces its antiarrhythmic effect by:

slowing intracardiac conduction, which slightly increases the duration of the action potential in atrial and ventricular muscle, thus prolonging the PR interval, QRS complex, and QT interval

shortening the action potential of Purkinje fibers without affecting surrounding myocardial tissue

inhibiting extracellular calcium influx (at high doses)

stopping paroxysmal reentrant supraventricular tachycardias by acting on antegrade pathways of dysfunctional AV conduction

decreasing conduction in accessory pathways in those with Wolff-Parkinson-White syndrome.

Contraindications

Cardiogenic shock, hypersensitivity to flecainide or its components, recent MI, right bundle-branch block associated with left hemiblock or secondor third-degree AV block unless pacemaker is present

Interactions

amiodarone: Increased blood flecainide level beta blockers, disopyramide, verapamil: Possibly myocardial depression and increased blood levels of both calcium channel blockers: Increased risk of arrhythmias digoxin: Possibly increased blood digoxin level urinary acidifiers: Possibly increased flecainide elimination and decreased therapeutic effects urinary alkalinizers: Possibly decreased flecainide elimination and increased therapeutic effects acidic juices, that decrease urine pH below 5.0: Increased flecainide elimination and decreased therapeutic effects that increase urine pH above 7.0, strict vegetarian diet: Decreased flecainide elimination and increased therapeutic effects smoking: Increased flecainide clearance

Side Efect

CNS: Anxiety, depression, dizziness, drowsiness, fatigue, headache, light-headedness, tremor, weakness flecainide acetate 442
CV: Arrhythmias, chest pain, heart failure, hypotension
EENT: Blurred vision
GI: Abdominal pain, anorexia, constipation, hepatic dysfunction, nausea, vomiting
RESP: Dyspnea
SKIN: Rash

Cautions

Monitor urine pH at the start of flecainide therapy.

Check blood pressure, fluid intake and output, and weight regularly during therapy.

Monitor trough flecainide level, as needed; therapeutic level is 0.2 to 1 mcg/ml.

Expect drug to cause mild to moderate negative inotropic effects, minimal cardiovascular effects, and no effect on blood pressure, heart rate, and left ventricular function.
WARNING Because hypokalemia or hyperkalemia may interfere with flecainide’s therapeutic effects, monitor serum potassium level before and during therapy and notify prescriber immediately if potassium imbalance develops. Also monitor for and notify prescriber about prolonged PR interval, QRS complex, or QT interval; chest pain; hypotension; and signs of heart failure. Keep in mind that drug can cause fatal proarrhythmias, which is why it isn’t considered a first-line antiarrhythmic.

Expect prolonged flecainide therapy to raise blood alkaline phosphatase level.

PATIENT SAFTY

Instruct patient to take flecainide at regular intervals to keep a constant blood level.

Advise patient to take a missed dose as soon as she remembers if it’s within 6 hours of the scheduled time.

Teach patient how to take her pulse, and instruct her to record it daily, along with her weight. Advise her to bring record to follow-up visits.

Encourage family members to obtain instruction in basic cardiac life support.

Advise patient to notify prescriber immediately about chest pain, difficulty breathing, and dizziness.

Caution patient not to stop taking flecainide suddenly but to taper dosage gradually according to prescriber’s instructions.

Category

Chemical class: Triazole derivative
Therapeutic class: Antifungal

Pregnancy category: C

Indications

To treat oral and esophageal candidiasis ORAL SUSPENSION,,
I.V.INJECTION Adults and adolescents. 200 mg on day 1 followed by 100 mg daily for at least 2 (oral) or 3 (esophageal) wk after symptoms resolve. Children.3 mg/kg daily for at least 2 (oral) or 3 (esophageal) wk and then for 2 wk after esophageal symptoms resolve. To treat systemic candidiasis ORAL SUSPENSION,,
I.V.INJECTION Adults and adolescents.400 mg on day 1, followed by 200 mg daily for at least 4 wk and then for additional 2 wk after symptoms resolve. To treat cryptococcal meningitis ORAL SUSPENSION,,
I.V.INJECTION Adults and adolescents.400 mg daily until patient responds to treatment, then 200 to 400 mg daily for 10 to 12 wk after CSF culture is negative. Maintenance: 200 mg daily to suppress relapse. Children.6 to 12 mg/kg daily for 10 to 12 wk after CSF culture is negative. To prevent candidiasis after bone marrow transplantation ORAL SUSPENSION,,
I.V.INJECTION Adults and adolescents.400 mg daily starting several days before procedure if severe neutropenia is expected and continued for 7 days after absolute neutrophil count exceeds 1,000/mm3. To treat vaginal candidiasis , ORAL SUSPENSION,
Adults. 150 mg as a single dose.
DOSAGE ADJUSTMENT Dosage reduced for patients with hepatic or renal impairment. Dosage reduced by 50% for patients with creatinine clearance of 11 to 50 ml/min/ 1.73 m2.

Mechanism of Action

Damages fungal cells by interfering with a cytochrome P-450 enzyme needed to confluconazole 443 E F vert lanosterol to ergosterol, an essential part of the fungal cell membrane. Decreased ergosterol synthesis causes increased cell permeability, which allows cell contents to leak. Fluconazole also may inhibit endogenous respiration, interact with membrane phospholipids, inhibit transformation of yeasts to mycelial forms, inhibit purine uptake, and impair biosynthesis of triglycerides and phospholipids.

Incompatibilities

Don’t add fluconazole to I.V. bag that contains any other drug.

Contraindications

Hypersensitivity to fluconazole or its components

Interactions

astemizole, terfenadine: Increased blood levels of these benzodiazepines (short-acting): Possibly increased benzodiazepine level and psychomotor effects
cimetidine: Decreased fluconazole level cisapride: Possibly increased QT interval, leading to torsades de pointes cyclosporine: Increased cyclosporine level glipizide, glyburide, tolbutamide: Increased risk of hypoglycemia hydrochlorothiazide: Increased fluconazole level from decreased excretion isoniazid,
rifampin: Decreased fluconazole effects nonsedating antihistamines: Increased blood antihistamine level, increased risk of cardiotoxicity oral anticoagulants: Increased anticoagulant effects
phenytoin: Increased phenytoin level
rifabutin: Increased rifabutin level
theophylline: Increased theophylline level zidovudine: Increased zidovudine level

Side Efect

CNS: Chills, dizziness, drowsiness, fever, headache, seizures
CV: Prolonged QT interval, torsades de pointes
GI: Abdominal pain, anorexia, constipation, diarrhea, hepatic failure, nausea, vomiting
HEME: Agranulocytosis, leukopenia, thrombocytopenia
SKIN: Exfoliative dermatitis, photosensitivity, pruritus, rash
Other: Anaphylaxis, angioedema

Cautions

Use fluconazole cautiously in patients with potentially proarrhythmic conditions because drug may prolong the QT interval, which can lead to life-threatening torsades de pointes.

Expect to obtain BUN and serum creatinine levels and culture and sensitivity and liver function test results before therapy starts.

Refrigerate, but don’t freeze, fluconazole oral suspension. Shake well before administering.

Discard I.V. solution that’s cloudy or contains precipitate. Don’t infuse more than 200 mg/hr or add supplemental to infusion.

Monitor hepatic and renal function periodically during therapy, and notify prescriber if you detect signs of dysfunction.

Assess for rash every 8 hours during therapy, and notify prescriber if rash occurs.

If patient receives an oral anticoagulant, monitor coagulation test results and assess patient for bleeding.

Monitor patient for symptoms of overdose, such as hallucinations and paranoia. If they occur, provide supportive treatment, gastric lavage, and, possibly, hemodialysis, which can reduce blood fluconazole level by half after about 3 hours.

PATIENT SAFTY

Instruct patient to take fluconazole tablets or oral suspension 30 minutes before or 2 hours after meals. Inform her that tablets may be crushed for easier swallowing if needed.

Advise patient to complete entire course of therapy, even if she feels better.

If patient takes an oral antidiabetic, urge her to monitor blood glucose level often because of increased risk of hypoglycemia.

Alert patient that fluconazole may change the taste of food.

Encourage patient to notify prescriber immediately about diarrhea, headache, nausea, rash, right-upper-quadrant abdominal pain, yellow skin or whites of eyes, or vomiting.

Suggest that breast-feeding patient consult prescriber because breast-feeding may need to be stopped during therapy.

Category

Chemical class: Glucocorticoid
Therapeutic class: Mineralocorticoid replacement

Pregnancy category: C

Indications

To treat primary and secondary chronic adrenocortical insufficiency Adults and adolescents.Usual: 100 mcg daily. Dosage may range from 100 mcg three times/wk to 200 mcg daily. Children.50 to 100 mcg daily. To treat salt-losing adrenogenital syndrome
Adults. 100 to 200 mcg daily. Children.50 to 100 mcg daily.
DOSAGE ADJUSTMENT Dosage reduced to 50 mcg daily if transient hypertension develops during therapy. Route Onset Peak Duration P.O. Unknown Unknown 1–2 days

Mechanism of Action

Enhances sodium reabsorption, hydrogen and potassium excretion, and water retention by the distal renal tubules, much like aldosterone, an endogenous mineralocorticoid. In large doses, fludrocortisone can inhibit endogenous adrenocortical secretion, thymic activity, and pituitary corticotropin excretion. It also can promote glycogen deposits in the liver and induce a negative nitrogen balance when protein intake is deficient.

Contraindications

Hypersensitivity to fludrocortisone, adrenocorticoids, or their components; systemic fungal infections

Interactions

digoxin: Increased risk of digitalis toxicity and arrhythmias from hypokalemia phenytoin,
rifampin: Decreased fludrocortisone effects potassium-wasting , such as loop diuretics and amphotericin B: Increased risk of severe hypokalemia

Side Efect

CNS: Dizziness, headache, mental changes, seizures
CV: Arrhythmias, heart failure, hypertension, peripheral edema
EENT: Cataracts (with long-term use), increased intraocular pressure
ENDO: Adrenal insufficiency, growth suppression in children, hyperglycemia
GI: Anorexia, nausea, vomiting
GU: Menstrual irregularities
HEME: Easy bruising
MS: Arthralgia, muscle weakness, myalgia, osteoporosis (with long-term use), tendon contractures
SKIN: Acne, diaphoresis, rash, urticaria
Other: Hypokalemia, hypokalemic alkalosis, impaired wound healing, weight gain

Cautions

Monitor blood pressure, fluid status, and serum electrolyte levels periodically during fludrocortisone therapy. Watch for signs of heart failure, including adventitious breath sounds, peripheral edema, and weight gain.

Monitor for signs and symptoms of overdose, such as cardiomegaly, edema, excessive weight gain, hypertension, and hypokalemia. These effects usually subside a few days after therapy stops. Potassium supplementation may be needed.

Notify prescriber if patient has dizziness, headache, hypertension, hypokalemia, signs of infection, or weight gain.

PATIENT SAFTY

Instruct patient to take a missed dose of fludrocortisone as soon as she remembers if it’s within 12 hours of scheduled time. Warn against double-dosing. Advise her to notify prescriber if she misses more than one dose or if nausea or vomiting prevents her from taking drug.

Instruct patient to reduce dietary sodium and to eat more potassium-rich during therapy.

Direct patient to weigh herself each morning before breakfast in clothes of similar weight and to notify prescriber if she gains more than 2 lb (0.9 kg) per day or 5 lb fludrocortisone acetate 445 E F (2.3 kg) per week. Instruct her to monitor how tightly her rings and shoes fit.

Advise patient to notify prescriber about stressful events, such as dental extractions, emotional upset, illness, surgery, and trauma; dosage increase may be required.

Instruct patient to notify prescriber about dizziness, fever, fluid retention, headache, joint pain, irregular heart rate, muscle weakness, or palpitations.

Inform patient that drug may delay wound healing.

Caution patient not to stop taking drug abruptly but to taper dosage gradually, as prescribed.

Urge patient to wear or carry medical identification that documents corticosteroid use.

Category

Chemical class: Imidazobenzodiazepine derivative
Therapeutic class: Benzodiazepine antidote

Pregnancy category: C

Indications

To reverse sedation from benzodiazepine therapy
I.V.INJECTION
Adults.0.2 mg, repeated after 45 to 60 sec if response is inadequate and then repeated every 1 min, if needed. If sedation recurs, regimen is repeated every 20 min or more. Maximum: 1 mg over 5 min or 3 mg over 1 hr. To reverse benzodiazepine toxicity or suspected overdose
I.V.INJECTION
Adults. 0.2 mg followed by 0.3 mg 30 to 60 sec later if response is inadequate and then 0.5 mg repeated every 1 min. If sedation recurs, regimen is repeated every 20 min. Maximum: 3 mg in 1-hr period.

Mechanism of Action

Antagonizes CNS effects of benzodiazepines by competing for their binding sites.

Contraindications

Evidence of tricyclic antidepressant overdose; hypersensitivity to flumazenil, benzodiazepines, or their components; use of benzodiazepine to control intracranial pressure, status epilepticus, or a potentially life-threatening condition Route Onset Peak Duration I.V. 1–2 min 6–10 min Variable

Interactions

benzodiazepines: Benzodiazepine withdrawal symptoms, including seizures nonbenzodiazepine agonists: Loss of effectiveness of these tetracyclic or tricyclic antidepressant overdose: High risk of seizures all : Increased flumazenil clearance (by half) with food ingestion during I.V. injection

Side Efect

CNS: Agitation, anxiety, ataxia, confusion, dizziness, drowsiness, emotional lability, fatigue, headache, hypoesthesia, insomnia, paresthesia, resedation, seizures, tremor, vertigo
CV: Hot flashes, hypertension, palpitations
EENT: Blurred vision, diplopia, dry mouth
GI: Nausea, vomiting
RESP: Dyspnea, hyperventilation, hypoventilation
SKIN: Diaphoresis, flushing, rash
Other: Injection site pain and thrombophlebitis

Cautions

Use flumazenil cautiously in patients with cardiac disease. Assess for increased stress or anxiety from benzodiazepine withdrawal because patient’s blood pressure may rise.

Give flumazenil undiluted or diluted in a syringe with D5W, normal saline solution, or lactated Ringer’s solution. Administer over 15 to 30 seconds directly into tubing of a free-flowing compatible I.V. solution. Use a large vein, if possible, to minimize pain at site. Avoid extravasation because drug may irritate tissue.

Be aware that drug may cause signs of benzodiazepine withdrawal in drugdependent patient. Also, abrupt awakening from benzodiazepine overdose can cause flumazenil 446 agitation, dysphoria, and increased adverse reactions.

Be aware that benzodiazepine reversal may cause an anxiety or a panic attack for patient with a history of these episodes. Expect to adjust dosage carefully.

Monitor patient for signs of resedation and hypoventilation for at least 2 hours after giving flumazenil because drug has a short half-life. Be aware that patient shouldn’t be discharged until the risk of resedation has resolved.

PATIENT SAFTY

Caution patient to avoid alcohol and OTC for 10 to 24 hours after taking drug.

Advise patient to avoid hazardous activities for 18 to 24 hours after discharge.

Inform patient and family that agitation, emotional lability, fear, and panic attack (if patient has a history of them) may occur. Tell them to seek medical care if patient has depression, trouble breathing, flushing, hyperventilation, insomnia, palpitations, or tremor.

Because drug doesn’t always reverse postprocedure amnesia, provide written instructions or instructions to caregiver even if patient is alert.

Category

Chemical class: Corticosteroid
Therapeutic class: Antiasthmatic, antiinflammatory

Pregnancy category: C

Indications

To provide maintenance treatment of asthma, alone or with oral corticosteroids INHALATION AEROSOL Adults and adolescents age 15 and over. 500 mcg (2 inhalations) b.i.d. morning and evening. Maximum: 2,000 mcg daily (4 inhalations b.i.d.). Children ages 6 to 15. 500 mcg (2 inhalations) b.i.d. Maximum: 1,000 mcg daily. To relieve symptoms of seasonal or perennial rhinitis NASAL SOLUTION
Adults. 50 mcg (2 sprays) b.i.d. in each nostril. Maximum: 400 mcg daily (16 sprays). Children.25 mcg (1 spray) t.i.d. in each nostril. Maximum: 200 mcg daily (8 sprays). Route Onset Peak Duration Inhalation In 4 wk Unknown Unknown Nasal 3–7 days Unknown 4–6 hr

Mechanism of Action

Inhibits cells involved in inflammatory response, such as mast cells, eosinophils, basophils, lymphocytes, macrophages, and neutrophils. Also inhibits production of chemical mediators, such as histamine, eicosanoids, leukotrienes, and cytokines.

Contraindications

Hypersensitivity to flunisolide or its components, primary treatment of status asthmaticus or other asthma episodes that require emergency care, recent nasal surgery (nasal form), untreated localized infection of nasal mucosa (nasal form)

Side Efect

CNS: Anxiety, chills, depression, dizziness, headache, hyperactivity, insomnia, irritability, lethargy, mood changes, nervousness, tremor, vertigo
CV: Hypertension
EENT: Candidiasis (oral and throat), dry mouth and throat, earache, eye infection, hoarseness, loss of smell or taste, mouth irritation, pharyngitis, rhinitis, sinusitis, sneezing
GI: Abdominal pain, anorexia, constipation, diarrhea, flatulence, heartburn, increased appetite, indigestion, nausea, vomiting
GU: Menstrual irregularities
HEME: Eosinophilia
RESP: Bronchitis, dyspnea, pleurisy, pneumonia
SKIN: Acne, eczema, pruritus, rash, urticaria
Other: Growth suppression (children), lymphadenopathy

Cautions

Use flunisolide cautiously in patients with ocular herpes simplex, pulmonary tuberculosis, or untreated systemic bacterial, fungal, parasitic, or viral infection.

If patient receives an oral corticosteroid, expect to taper it slowly 1 week after changing to flunisolide. For patient who flunisolide 447 E F receives prednisone, expect to reduce it by no more than 2.5 mg daily at weekly intervals, beginning at least 1 week after flunisolide therapy starts.
WARNING Assess patient switched from systemic corticosteroid to flunisolide for adrenal insufficiency (fatigue, hypotension, lassitude, nausea, vomiting, weakness) during initial treatment and during stress, trauma, surgery, infection, or other electrolyte-depleting conditions. Notify prescriber immediately if signs or symptoms arise.

Monitor growth in children; corticosteroids may increase risk of growth suppression.

PATIENT SAFTY

Teach patient how to use inhaler. When starting a new canister, advise spraying once into the air (avoiding her eyes) to check for mist.

Instruct patient to gargle or rinse after each use of flunisolide to help prevent mouth and throat dryness, relieve throat irritation, and prevent oropharyngeal infection.

Urge patient to contact prescriber if symptoms haven’t improved after 3 weeks.
WARNING Caution patient not to use flunisolide to relieve acute bronchospasm.

If patient switches from an oral corticosteroid to flunisolide, advise her to carry medical identification indicating the need for supplemental systemic corticosteroids during stress or severe asthma attack. Advise her to ask prescriber how to respond to these problems.

Caution patient to avoid exposure to chickenpox and measles and to contact prescriber immediately if exposure occurs.

Category

Chemical class: Phenylpropylamine derivative
Therapeutic class: Antibulimic, antidepressant, antiobsessive-compulsive

Pregnancy category: C

Indications

To treat depression ,,(PROZAC)
Adults. Initial: 20 mg daily in the morning. Dosage increased every 4 to 8 wk as needed. Dosage greater than 20 mg daily given b.i.d. morning and noon. Maximum: 80 mg daily. Children and adolescents. Initial: 10 mg daily. Increased after 1 wk to 20 mg daily.
DOSAGE ADJUSTMENT For lower-weight children, dosage increased to 20 mg daily only if improvement insufficient after several wk. DELAYED-RELEASE (PROZAC WEEKLY)
Adults.90 mg/wk, beginning 7 days after last 20-mg daily dose. To treat obsessive-compulsive disorder ,,(PROZAC)
Adults.Initial: 20 mg daily in the morning. Dosage increased every 4 to 8 wk as needed. Dosage greater than 20 mg daily given b.i.d. morning and noon. Maximum: 80 mg daily. Children and adolescents. Initial: 10 mg daily. Dosage increased after 2 wk to 20 mg daily. Subsequent dosage increased, as needed, at intervals of at least several wk. Maintenance: 20 to 60 mg daily.
DOSAGE ADJUSTMENT For lower-weight children, dosage should be increased above 10 mg daily only if clinical improvement remains insufficient after several wk. Maintenance dosage for such patients should not exceed 30 mg daily. To treat moderate to severe bulimia nervosa ,,(PROZAC)
Adults.60 mg daily in the morning. Some patients may be prescribed a lower dose, which is titrated to 60 mg daily as tolerated. To treat panic disorder with or without agoraphobia ,,(PROZAC)
Adults.Initial: 10 mg daily. Dosage increased in 1 wk to 20 mg daily, as needed. Maximum: 60 mg daily. To treat premenstrual dysmorphic disorder (SARAFEM)
Adults.20 mg daily. Dosage increased as needed. Maximum: 80 mg daily.
DOSAGE ADJUSTMENT Dose or frequency reduced for patients with hepatic impairfluoxetine hydrochloride 448 ment or concurrent illness, those who take multiple medications, and for elderly patients. Route Onset Peak Duration P.O.* 1–6 wk Unknown Unknown

Mechanism of Action

Selectively inhibits reuptake of the neurotransmitter serotonin by CNS neurons and increases the amount of serotonin available in nerve synapses. An elevated serotonin level may result in elevated mood and, consequently, reduced depression.

Contraindications

Hypersensitivity to selective serotonin reuptake inhibitors or their components, use within 14 days of MAO inhibitor therapy

Interactions

alprazolam, diazepam: Possibly prolonged half-life of these aspirin, NSAIDs,
warfarin: Increased anticoagulant activity and risk of bleeding astemizole: Increased risk of serious arrhythmias buspirone: Decreased buspirone effects clozapine, fluphenazine, haloperidol, maprotiline, trazodone: Increased risk of adverse effects CYP2D6-metabolized , such as antiarrhythmics (especially flecainide, propafenone), selected antidepressants (tricyclics), antipyschotics (phenothiazines and most atypicals), thioridazine, and vinblastine: Increased plasma levels of these and increased risk of serious

Side Efect

linezolid, lithium, serotonergics (such as amphetamines and other psychostimulants, antidepressants, and dopamine agonists), St. John’s wort, tramadol, triptans: Increased risk of serotonin syndrome
MAO inhibitors: Possibly severe and lifethreatening adverse effects
phenytoin: Increased blood phenytoin level and risk of toxicity pimozide: Possibly bradycardia sumatriptan: Increased risk of weakness, hyperreflexia, and difficulty with coordination tryptophan: Increased risk of central and peripheral toxicity

Side Efect

CNS: Anxiety, chills, dream disturbances, drowsiness, fatigue, fever, headache, hypomania, insomnia, mania, nervousness, neuroleptic malignant syndrome, restlessness, seizures, serotonin syndrome, somnolence, suicidal ideation, tremor, vertigo, weakness, yawning
CV: Hypotension, palpitations
EENT: Abnormal vision, dry mouth, pharyngitis, sinusitis
ENDO: Galactorrhea, gynecomastia, hypoglycemia, syndrome of inappropriate antidiuretic hormone secretion (SIADH)
GI: Anorexia, diarrhea, indigestion, nausea
GU: Decreased libido, ejaculation disorders, impotence
HEME: Altered platelet function, unusual bleeding
MS: Arthralgia, myalgia
RESP: Dyspnea
SKIN: Diaphoresis, pruritus, rash, urticaria
Other: Flulike symptoms, hyponatremia, weight loss

Cautions

Use fluoxetine cautiously in patients with a history of seizures.
WARNING Avoid giving fluoxetine within 14 days of an MAO inhibitor or starting MAO inhibitor therapy within 5 weeks of discontinuing fluoxetine.

In patients taking fluoxetine for depression (especially children, adolescents, and young adults), watch closely for suicidal tendencies, particularly when therapy starts and dosage changes, because depression may worsen temporarily during those times.

Monitor patient closely for evidence of GI bleeding, especially if patient takes another drug known to increase the risk, such as aspirin, an NSAID, or warfarin.

Monitor patient—especially an elderly patient—for hypoosmolarity of serum and urine and for hyponatremia (headache, difficulty concentrating, memory impairment, weakness, unsteadiness), which may indicate fluoxetine-induced SIADH.

To discontinue, expect to taper drug, as ordered, to minimnize

Side Efect

. fluoxetine hydrochloride 449 E F * Capsules, oral solution, and tablets. For depression and bulimia; 5 wk for obsessive-compulsive disorder.
WARNING Monitor patient for possible serotonin syndrome, characterized by agitation, chills, confusion, diaphoresis, diarrhea, fever, hyperactive reflexes, poor coordination, restlessness, shaking, talking or acting with uncontrolled excitement, tremor, and twitching, especially if patient is receiving another drug that raises serotonin level (such as dopamine agonist, MAO inhibitor, tryptophan, amphetamine, and other antidepressant or psychostimulant). In its most severe form, serotonin syndrome can resemble neuroleptic malignant syndrome, which includes a high fever, muscle rigidity, autonomic instability, and possible fluctuations in vital signs and mental status.

Monitor patient with diabetes mellitus for altered blood glucose level because drug may cause hypoglycemia during therapy and hyperglycemia when it stops. Expect to adjust dosage of antidiabetic drug, as prescribed.

Expect patient to be reevaluated periodically to determine continued need for therapy.

When stopping fluoxetine therapy, expect to taper drug to minimize adverse reactions.

PATIENT SAFTY

WARNING Tell patient that drug increases risk of serotonin syndrome, a rare but serious complication, especially when taken with certain other . Teach patient to recognize its signs and symptoms, and advise her to notify prescriber immediately if they occur.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes and particularly if patient is a child, teenager, or young adult.

Caution patient to avoid hazardous activities until CNS effects of drug are known.

Caution against stopping fluoxetine abruptly because serious adverse effects may result.

Advise patient to consult prescriber before taking OTC or prescription , if a rash or hives develop, or if she becomes or intends to become pregnant during therapy.

Inform patient that drug may take several weeks to achieve full effects.

Category

Chemical class: Phenothiazine, propylpiperazine derivative
Therapeutic class: Antipsychotic

Pregnancy category: Not rated

Indications

To control psychotic disorders ELIXIR,,(FLUPHENAZINE HYDROCHLORIDE) Adults and adolescents.Initial: 2.5 to 10 mg/day in divided doses every 6 to 8 hr. When symptoms are controlled, dosage reduced to 1 to 5 mg daily. Maximum: 20 mg/dose with caution. Children. 250 to 750 mcg once daily to q.i.d.
I.M.INJECTION(FLUPHENAZINE HYDROCHLORIDE) Adults and adolescents. Initial: 1.25 mg, increased as clinical condition tolerates up to 2.5 to 10 mg daily in divided doses every 6 to 8 hr. Maximum: 10 mg daily.
DOSAGE ADJUSTMENT For elderly or debilitated patients, dosage reduced to 1 to 2.5 mg daily in divided doses every 6 to 8 hr. I.M.OR SUBCUTANEOUS INJECTION(FLUPHENAZINE DECANOATE OR ENANTHATE)
Adults.Initial: 12.5 to 25 mg every 1 to 4 wk, as needed (decanoate). For doses over 50 mg, next dose increased cautiously by 12.5 mg. Or 25 mg every 2 wk, with dose and dosing interval adjusted based on patient response (enanthate). Maximum: 100 mg/dose. fluphenazine 450 Adolescents and children age 12. Initial: 6.25 to 18.75 mg/wk (decanoate), increased to 12.5 to 25 mg every 1 to 3 wk, according to condition. Children ages 5 to 12. 3.125 to 12.5 mg every 1 to 3 wk (decanoate), according to condition. Route Onset Peak Duration P.O. In 1 hr Variable 6–8 hr I.M.* In 1 hr Variable 6–8 hr I.M., In 24– Variable 1–6 wk SubQ 72 hr

Mechanism of Action

May block postsynaptic dopamine receptor sites in the CNS. This action may depress areas of the brain that control activity and aggression, including the cerebral cortex, hypothalamus, and limbic system.

Incompatibilities

Don’t mix fluphenazine hydrochloride oral solution with beverages that contain caffeine, such as coffee and cola; tannins, such as tea; or pectins, such as apple juice. They’re physically incompatible.

Contraindications

Blood dyscrasias, bone marrow depression, cerebral arteriosclerosis, coma, concomitant use of large amounts of another CNS depressant, coronary artery disease, hepatic dysfunction, hypersensitivity to phenothiazines, myeloproliferative disorders, severe CNS depression, severe hypertension or hypotension, subcortical brain damage

Interactions

adsorbent antidiarrheals, aluminumor magnesium-containing antacids: Possibly inhibited absorption of fluphenazine amantadine, anticholinergics: Possibly intensified adverse effects of both amphetamines: Possibly decreased therapeutic effects of both antihypertensives: Possibly severe hypotension antithyroid : Increased risk of agranulocytosis
beta blockers: Possibly increased blood levels and risk of adverse effects of both bromocriptine: Decreased bromocriptine effects
CNS depressants: Possibly prolonged and intensified CNS depression erythromycin: Possibly inhibited fluphenazine metabolism guanethidine: Decreased hypotensive effect of guanethidine levodopa: Possibly decreased antidyskinetic effect of levodopa lithium: Possibly neurotoxicity (disorientation, extrapyramidal reactions, unconsciousness) meperidine: Excessive sedation and hypotension metrizamide: Increased risk of seizures when injected in subarachnoid area during fluphenazine therapy oral anticoagulants: Possibly decreased anticoagulant effects pimozide, other that prolong QT interval: Prolonged QT interval and risk of arrhythmias thiazide diuretics: Increased risk of hyponatremia, hypotension, and water intoxication tricyclic antidepressants: Possibly prolonged and intensified sedation
alcohol use: Possibly increased CNS depression and increased risk of heatstroke

Side Efect

CNS: Ataxia, cerebral edema, dizziness, drowsiness, headache, insomnia, lightheadedness, nervousness, seizures, slurred speech, syncope, worsening psychotic symptoms
CV: AV conduction disorders, bradycardia, cardiac arrest, hypercholesterolemia, hypertension, orthostatic hypotension, QT-interval prolongation, shock, ST-segment depression, tachycardia
EENT: Blurred vision, dry mouth, glaucoma, increased salivation, laryngeal edema, laryngospasm, miosis, mydriasis, nasal congestion, papillary hypertrophy of the tongue, parotid gland enlargement, photophobia, pigmentary retinopathy, ptosis
ENDO: Breast engorgement (females), galactorrhea, hyperglycemia, hypoglycemia, mastalgia, syndrome of inappropriate ADH secretion fluphenazine 451 E F * For hydrochloride. For decanoate and enanthate. For decanoate; 2 wk for enanthate.
GI: Anorexia, constipation, diarrhea, fecal impaction, ileus, increased appetite, nausea, vomiting
GU: Amenorrhea, bladder paralysis, decreased libido, enuresis, menstrual irregularities, polyuria, urinary frequency, urinary incontinence, urine retention
HEME: Anemia, aplastic anemia, eosinophilia, leukopenia, thrombocytopenia, thrombocytopenic or nonthrombocytopenic purpura
RESP: Bronchospasm, dyspnea, increased respiratory depth
SKIN: Contact dermatitis, dry skin, eczema, erythema, jaundice, photosensitivity, pruritus, seborrhea
Other: Heatstroke, hyponatremia, lupuslike symptoms, weight gain

Cautions

Fluphenazine shouldn’t be used to treat dementia-related psychosis in elderly patients because of an increased mortality risk.

Use fluphenazine cautiously in patients with a history of glaucoma or renal impairment.

For I.M. and subcutaneous injection, use at least a 21G needle.

Monitor temperature; a significant, unexplained rise can indicate intolerance and a need to discontinue drug. Notify prescriber immediately if this occurs.

Watch for signs of hepatic failure, such as jaundice.

Notify prescriber about worsening psychotic sympto
MS: agitation, catatonic state, confusion, depression, hallucinations, lethargy, paranoid reactions.

PATIENT SAFTY

If patient takes elixir form of fluphenazine, instruct her to keep it in an amber or opaque bottle because drug is sensitive to light.

Advise patient not to mix oral solution with beverages that contain caffeine (coffee, cola), tannins (tea), or pectins (apple juice).

Caution patient about possible dizziness or light-headedness.

Teach patient how to prevent heatstroke, orthostatic hypotension, and photosensitivity reactions.

Warn against stopping drug abruptly.

Category

Chemical class: Benzodiazepine
Therapeutic class: Sedative-hypnotic

Pregnancy category: Not rated

Controlled substance schedule: IV

Indications

To treat insomnia characterized by difficulty falling asleep, frequent nocturnal awakenings, or early-morning awakening
Adults.15 to 30 mg at bedtime.
DOSAGE ADJUSTMENT Initial dose reduced to 15 mg for elderly or debilitated patients until individual response is known. Route Onset Peak Duration P.O. 15–45 min Unknown 7–8 hr

Mechanism of Action

May potentiate the effects of gammaaminobutyric acid (GABA) and other inhibitory neurotransmitters by binding to specific benzodiazepine receptor sites in the limbic and cortical areas of the CNS. As a result, flurazepam increases GABA’s inhibitory effects and blocks cortical and limbic arousal.

Contraindications

Acute angle-closure glaucoma, breastfeeding, hypersensitivity to other benzodiazepines, itraconazole or ketoconazole therapy, psychosis

Interactions

cimetidine, diltiazem, disulfiram, erythromycin, fluoxetine, fluvoxamine, itraconazole, nefazodone, estrogen-containing oral contraceptives, propoxyphene, ranitidine, verapamil: Possibly increased blood level and impaired hepatic metabolism of flurazepam clozapine: Possibly cardiac arrest or respiratory depression
CNS depressants: Possibly potentiated CNS flurazepam hydrochloride 452 depression levodopa: Possibly decreased therapeutic effects of levodopa grapefruit juice: Possibly increased blood level and impaired hepatic metabolism of flurazepam
alcohol use: Possibly potentiated CNS and respiratory depression

Side Efect

CNS: Amnesia, anxiety, ataxia, bizarre behavior (such as sleep driving), confusion, delusions, depression, dizziness, drowsiness, euphoria, headache, hypokinesia, irritability, malaise, nervousness, slurred speech, tremor
CV: Chest pain, palpitations, tachycardia
EENT: Blurred vision, dry mouth, increased salivation, photophobia
GI: Abdominal pain, constipation, diarrhea, nausea, thirst, vomiting
GU: Libido changes
SKIN: Diaphoresis
Other: Anaphylaxis, angioedema, physical or psychological dependence

Cautions

Use flurazepam cautiously in patients with severe mental depression or reduced respiratory function; drug may intensify mental depression and lead to respiratory depression.

Expect to use lowest effective dose in elderly or debilitated patients to minimize the risk of ataxia, confusion, dizziness, and oversedation.

Monitor liver function test results, as appropriate.

PATIENT SAFTY

Instruct patient not to exceed prescribed dosage and not to stop drug abruptly.
WARNING Warn patient that, although rare, drug may cause swelling of the oral cavity or throat, which could cause airway obstruction. If swelling occurs, patient should seek emergency care immediately and never take flurazepam again.

Caution patient about possible morning dizziness or drowsiness.

Because flurazepam can reduce alertness, advise patient to avoid hazardous activities until drug’s CNS effects are known.

Caution patient to avoid alcohol and CNS depressants during therapy.

Advise patient to notify prescriber if she becomes or intends to become pregnant during therapy.

Inform patient that sleep may be disturbed for the first few nights after stopping drug.

Warn patient and caregiver that some patients have performed bizarre activities after taking drug, such as driving their car, preparing and eating food, making phone calls, or having sex while not fully awake and often with no memory of the event. These episodes usually occur in patients who have taken the drug with alcohol or other CNS depressant or who have exceeded the recommended dose. If such an episode occurs, the prescriber should be notified and flurazepam therapy discontinued immediately.

Category

Chemical class: Propionic acid derivative
Therapeutic class: Antiarthritis, antiinflammatory

Pregnancy category: B

(first trimester), Not rated (later trimesters)

Indications

To treat acute or chronic rheumatoid arthritis and osteoarthritis
Adults. 200 mg daily in the evening.
Adults. Initial: 200 to 300 mg daily in divided doses b.i.d. to q.i.d. Maximum: 300 mg daily (100 mg/dose).

Mechanism of Action

Blocks the activity of cyclooxygenase, the enzyme necessary for prostaglandin synthesis. Prostaglandins, important mediators in the inflammatory response, cause local vasodilation with swelling and pain. They also play a role in pain transmission from the periphery to the spinal cord. By blocking cyclooxygenase and inhibiting prostaglandins, this NSAID causes inflammatory symptoms and pain to subside. flurbiprofen 453 E F

Contraindications

Angioedema, asthma, bronchospasm, nasal polyps, rhinitis, or urticaria induced by aspirin, iodides, or NSAIDs; hypersensitivity to NSAIDs

Interactions

acetaminophen: Increased risk of renal impairment with long-term use of both antacids: Decreased flurbiprofen effectiveness anticoagulants, cefamandole, cefoperazone, cefotetan, heparin, plicamycin, thrombolytics,
valproic acid: Increased risk of bleeding antineoplastics: Increased adverse hematologic effects cyclosporine: Increased risk of nephrotoxicity diuretics, triamterene: Decreased effectiveness of these glucocorticoids, other NSAIDs, potassium supplements: Increased adverse GI effects insulin, oral antidiabetic : Increased risk of hypoglycemia lithium: Increased risk of lithium toxicity methotrexate: Increased risk of methotrexate toxicity salicylates: Increased risk of GI bleeding alcohol use, smoking: Increased risk of GI bleeding

Side Efect

CNS: Anxiety, cerebral hemorrhage, depression, dizziness, drowsiness, forgetfulness, headache, insomnia, malaise, nervousness, stroke, tremor, weakness
CV: Arrhythmias, heart failure, hypertension, hypotension, palpitations, peripheral edema, tachycardia
EENT: Amblyopia, blurred vision, rhinitis, stomatitis, tinnitus, vision changes
GI: Abdominal cramps or distress, anorexia, constipation, diarrhea, diverticulitis, dysphagia, esophagitis, flatulence, gastritis, gastroenteritis, gastroesophageal reflux disease, GI bleeding or ulceration, hemorrhoids, hiatal hernia, hepatitis, increased appetite, indigestion, jaundice, liver failure, melena, nausea, perforation of stomach or intestines, stomatitis, vomiting
GU: Hematuria, interstitial nephritis, renal failure, UTI
HEME: Agranulocytosis, aplastic anemia, eosinophilia, leukopenia, neutropenia, pancytopenia, thrombocytopenia
SKIN: Erythema multiforme, exfoliative dermatitis, flushing, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, angioedema, hyponatremia

Cautions

Use flurbiprofen with extreme caution in patients who have a history of ulcer disease or GI bleeding because NSAIDs such as flurbiprofen increase the risk of GI bleeding and ulceration. Expect to use flurbiprofen for the shortest time possible in these patients.

Be aware that serious GI tract ulceration, bleeding, and perforation may occur without
WARNING signs or symptoms. Elderly patients are at greater risk. To minimize the risk, give flurbiprofen with food. If GI distress occurs, withhold drug and notify prescriber immediately.

Use flurbiprofen cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.
WARNING Monitor patient closely for thrombotic events, including MI and stroke, because NSAIDs increase the risk.

Monitor patient—especially if she’s elderly or receiving long-term flurbiprofen therapy—for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results because, rarely, elevations may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in elderly patients, patients taking diuretics or ACE inhibitors, and patients with heart failure, impaired renal function, or hepatic dysfunction; flurbiprofen may cause renal failure.

Monitor CBC for decreased hemoglobin and hematocrit because drug may worsen anemia.
WARNING If patient has bone marrow suppression or is receiving an antineoplastic drug, monitor laboratory results (including WBC count), and watch for evidence of infection because anti-inflammatory flurbiprofen 454 and antipyretic actions of flurbiprofen may mask signs and symptoms, such as fever and pain.

Assess patient’s skin regularly for signs of rash or other hypersensitivity reaction because flurbiprofen is an NSAID and may cause serious skin reactions without
WARNING, even in patients with no history of NSAID sensitivity. At first sign of reaction, stop drug and notify prescriber.

PATIENT SAFTY

Encourage patient to take flurbiprofen with food or milk to avoid GI distress.

Caution patient about possible blurred vision, dizziness, and drowsiness.

Advise patient to avoid aspirin, alcohol, and smoking during flurbiprofen therapy.

Urge patient to notify prescriber immediately if she has blood in urine, easy bruising, itching, rash, swelling, or yellow eyes or skin.

Caution pregnant patient not to take NSAIDs such as flurbiprofen during the last trimester because they may cause premature closure of the ductus arteriosus.

Explain that flurbiprofen may increase the risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.

Explain that flurbiprofen may increase the risk of serious adverse GI reactions; stress the importance of seeking immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.

Alert patient to rare but serious skin reactions. Urge her to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity.

Category

Chemical class: Trifluorinated corticosteroid
Therapeutic class: Antiasthmatic, antiinflammatory

Pregnancy category: C

Indications

To prevent asthma attacks, alone or with oral corticosteroids INHALATION AEROSOL Adults and children age 12 and over using bronchodilator therapy.Initial: 88 mcg inhaled b.i.d. Maximum: 440 mcg inhaled b.i.d. Adults and children age 12 and over switching from another inhaled corticosteroid.Initial: 88 to 220 mcg inhaled b.i.d. Maximum: 440 mcg inhaled b.i.d. Adults and children age 12 and over using oral corticosteroid therapy. Initial and maximum: 880 mcg inhaled b.i.d. Children ages 4 to 11 regardless of previous therapy. 88 mcg b.i.d. Maximum: 88 mcg b.i.d. To prevent seasonal or perennial allergic rhinitis NASAL SUSPENSION (FLONASE) Adults and children age 12 and over. Initial: 100 mcg (2 sprays) in each nostril daily or 50 mcg (1 spray) in each nostril b.i.d, as needed. Maintenance: 50 mcg (1 spray) in each nostril daily, as tolerated and needed. Maximum: 200 mcg daily (4 sprays). Children ages 4 to 11. 50 or 100 mcg (1 or 2 sprays) in each nostril daily in the morning, as needed. Maximum: 200 mcg daily (4 sprays). To treat seasonal or perennial allergic rhinitis NASAL SUSPENSION (FLONASE) Adults and children age 12 and over. Initial: 100 mcg (2 sprays) in each nostril daily or 50 mcg (1 spray) in each nostril b.i.d, as needed. Maintenance: 50 mcg (1 spray) in each nostril daily, as tolerated and needed. Maximum: 200 mcg daily (4 sprays). Children ages 4 to 11. 50 or 100 mcg (1 or 2 sprays) in each nostril daily in the morning, as needed. Maximum: 200 mcg daily (4 sprays). NASAL SUSPENSION(VERAMYST) Adults and children age 12 and over. fluticasone 455 E F Initial: 110 mcg (2 sprays) in each nostril once daily, decreasedto 55 mcg (1 spray) in each nostril once daily when symptoms are controlled. Maintenance: 55 mcg (1 spray) in each nostril once daily. Children ages 2 to 11. Initial: 55 mcg (1 spray) in each nostril once daily, increased to 110 mcg (2 sprays) in each nostril once daily, as needed. Maintenance: 55 mcg (1 spray) in each nostril once daily. Route Onset Peak Duration InhalaIn 24 hr 1–2 wk Several tion days Nasal 12 hr– 4–7 1–2 wk 3 days days

Mechanism of Action

Inhibits cells involved in the inflammatory response of asthma, such as mast cells, eosinophils, basophils, lymphocytes, macrophages, and neutrophils. Fluticasone also inhibits production or secretion of chemical mediators, such as histamine, eicosanoids, leukotrienes, and cytokines.

Contraindications

Hypersensitivity to fluticasone or its components, primary treatment of status asthmaticus or other acute asthma episodes that require intensive measures, untreated nasal mucosal infection (nasal suspension)

Interactions

ketoconazole, ritonavir and other strong cytochrome P-450 3A4 inhibitors (long-term use): Possibly increased fluticasone level and decreased serum cortisol level

Side Efect

CNS: Aggressiveness, agitation, depression, difficulty speaking, dizziness, fatigue, fever, headache, insomnia, malaise, restlessness
EENT: Allergic rhinitis, cataracts, conjunctivitis, dry mouth and throat, eye irritation, glaucoma, hoarseness, laryngitis, loss of voice, nasal congestion or discharge, nasal sinus pain, oropharyngeal candidiasis, otitis media, pharyngitis, sinusitis, throat irritation, tonsillitis
ENDO: Adrenal insufficiency, cushingoid symptoms, hyperglycemia, slower growth in children
GI: Abdominal pain, diarrhea, indigestion, nausea, vomiting
GU: Dysmenorrhea
HEME: Churg-Strauss syndrome, easy bruising, eosinophilia
MS: Arthralgia, myalgia, osteoporosis
RESP: Asthma exacerbation, bronchitis, bronchospasm, chest congestion and tightness, cough, dyspnea, pneumonia, upper respiratory tract infection, wheezing
SKIN: Dermatitis, ecchymosis, pruritus, rash, urticaria
Other: Anaphylaxis, angioedema, flulike symptoms, weight gain

Cautions

Use fluticasone cautiously in patients with ocular herpes simplex, pulmonary tuberculosis, or untreated systemic bacterial, fungal, parasitic, or viral infection.

Although anaphylaxis is rare, monitor patient closely at start of therapy, especially if patient has severe allergy to milk. If hypersensitivity reaction occurs, notify prescriber, expect drug to be discontinued, and provide supportive care, as prescribed.

If patient takes a systemic corticosteroid, expect to taper dosage by no more than 2.5 mg daily at weekly intervals, starting 1 week after fluticasone therapy begins.
WARNING If patient is switched from systemic corticosteroid to fluticasone, assess for adrenal insufficiency (fatigue, hypotension, lassitude, nausea, vomiting, weakness) early in therapy and when patient has infection, stress, trauma, surgery, or other electrolyte-depleting conditions or procedures. Notify prescriber immediately if signs or symptoms develop.

As prescribed, administer a fast-acting inhaled bronchodilator if bronchospasm occurs immediately after fluticasone use. Expect to stop fluticasone and start another drug therapy.

Expect to titrate fluticasone to lowest effective dosage after asthma has stabilized.

PATIENT SAFTY

Urge patient to use fluticasone regularly, as prescribed, not for acute bronchospasm.

Teach patient how to administer drug according to the form prescribed (nasal spray or oral inhaler).

Instruct patient to shake canister and use inhaler according to package instructions. On first use, advise her to spray 4 times fluticasone 456 into the air (away from her eyes and shaking inhaler between each test spray) and look for a fine mist. If inhaler hasn’t been used for more than 7 days or it’s dropped, it will need to be primed again by shaking well and then releasing 1 test spray into the air (away from her face).

If 2 inhalations are prescribed, tell patient to wait at least 1 minute between them.

Instruct patient to gargle and rinse her mouth after each dose to help prevent dry mouth and throat, relieve throat irritation, and prevent oropharyngeal yeast infection.

If patient uses more than 1 inhaler, instruct her to use fluticasone last, at least 5 minutes after previous inhaler.

Instruct patient to clean inhaler according to manufacturer guidelines at least once a week after her evening dose.

Inform patient that, when counter reads 020, she should obtain a refill, if needed. When counter reaches 000, she should discard the inhaler.

Instruct patient using
NASAL SPRAY to shake container well before each use.

Explain that symptoms may improve within 2 days but that full improvement may not occur for 1 to 2 weeks or longer.

Caution patient not to increase dosage but to contact prescriber after 1 week if symptoms continue or worsen.

Urge patient to tell prescriber immediately if asthma attacks don’t respond to bronchodilators during fluticasone therapy.

If patient is switching from an oral corticosteroid to fluticasone, urge her to carry medical identification indicating the need for supplemental systemic corticosteroids during stress or severe asthma attack.

Caution patient to avoid people who have infections because fluticasone suppresses the immune system, increasing the risk of infection. Instruct patient to notify prescriber about exposure to chickenpox, measles, or other infections because additional treatment may be needed.

Category

Chemical class: Heptenoic acid derivative
Therapeutic class: Antihyperlipidemic

Pregnancy category: X

Indications

As adjunct to lower cholesterol level in primary hypercholesterolemia, to decrease progression of coronary atherosclerosis, to reduce risk in patients with coronary artery disease undergoing coronary revascularization
Adults.20 to 40 mg daily in the evening or 40 mg b.i.d. Maximum: 40 mg b.i.d.
Adults. 80 mg in the evening. Maximum: 80 mg daily. As adjunct to lower cholesterol level in children with heterozygous familial hypercholesterolemia Girls ages 10 to 16 who are at least 1 year past menarche.Initial: 20 mg once daily, increased every 6 wk, as needed. Maximum: 40 mg b.i.d.
DOSAGE ADJUSTMENT For pediatric patients, if maximum dose of 40 mg b.i.d. is reached with immediate-release capsules, child may be switched to extended-release tablets, 80 mg once daily. Route Onset Peak Duration P.O. In 1–2 wk In 4–6 wk Unknown P.O. In 2 wk In 4 wk Unknown ()

Mechanism of Action

Interferes with the hepatic enzyme hydroxymethylglutaryl-coenzyme A reductase, reducing formation of mevalonic acid (a cholesterol precursor) and interrupting the pathway by which cholesterol is synthesized. When cholesterol level declines in hepatic cells, LDLs are consumed, which reduces circulating total cholesterol and serum triglycerides.

Contraindications

Acute hepatic disease, breast-feeding, hypersensitivity to fluvastatin or its components, pregnancy, unexplained persistently elevated liver enzyme levels

Interactions

bile acid sequestrants: Possibly decreased fluvastatin sodium 457 E F fluvastatin bioavailability cimetidine, omeprazole, ranitidine: Significantly increased blood fluvastatin level colchicine, cyclosporine, erythromycin, gemfibrozil, niacin: Increased risk of severe myopathy and rhabdomyolysis cyclosporine, erythromycin, gemfibrozil, niacin: Increased risk of acute renal failure fluconazole: Increased fluconazole level itraconazole,
ketoconazole: Increased risk of myopathy oral contraceptives: Risk of bleeding
rifampin: Significantly decreased blood fluvastatin level, increased plasma clearance
alcohol use: Increased bioavailability and blood level of fluvastatin

Side Efect

CNS: Dizziness, fatigue, headache, insomnia, weakness
EENT: Pharyngitis, rhinitis, sinusitis
GI: Abdominal cramps and pain, constipation, diarrhea, flatulence, indigestion, nausea, vomiting
GU: UTI
MS: Arthritis, back pain, myalgia, myositis, rhabdomyolysis
RESP: Bronchitis, cough, upper respiratory tract infection
SKIN: Pruritus, rash

Cautions

WARNING Expect to stop drug if CK level rises sharply or myopathy is suspected.

PATIENT SAFTY

Urge patient to comply with monthly laboratory tests early in treatment.

Tell patient to follow prescribed low-fat diet.

Encourage patient to notify prescriber promptly about muscle pain or unexplained weakness.

Category

Chemical class: Aralkylketone derivative
Therapeutic class: Antiobsessional

Pregnancy category: C

Indications

To treat obsessive-compulsive disorder
Adults.Initial: 50 mg at bedtime, increased by 50 mg every 4 to 7 days, if needed. Maximum: 300 mg daily. Children ages 8 to 17. Initial: 25 mg at bedtime, increased by 25 mg every 4 to 7 days, if needed. Maximum: 200 mg daily.
DOSAGE ADJUSTMENT Doses divided for adults taking more than 100 mg daily and for children taking more than 50 mg daily; given in 2 equal doses b.i.d. or in 2 unequal doses with the larger dose at bedtime.
Adults.Initial: 100 mg at bedtime, increased by 50 mg weekly, if needed. Maximum: 300 mg daily.
DOSAGE ADJUSTMENT For elderly patients or those with hepatic impairment, dosage increases with extended-release form are made more slowly. To treat social anxiety disorder
Adults. Initial: 100 mg at bedtime, increased by 50 mg weekly, if needed. Maximum: 300 mg daily.
DOSAGE ADJUSTMENT For elderly patients or those with hepatic impairment, dosage increases with extended-release form are made more slowly. Route Onset Peak Duration P.O. 3–10 wk Unknown Unknown

Mechanism of Action

May potentiate serotonin’s action by blocking its reuptake at neuronal membranes. An elevated serotonin level may elevate mood and decrease depression and anxiety, which often accompany obsessive-compulsive disorder.

Contraindications

Alosetron, astemizole, cisapride, pimozide, terfenadine, thioridazine, or tizanidine therapy, hypersensitivity to fluvoxamine maleate or its components, use within 14 days of MAO inhibitor

Interactions

alosetron: Increased plasma alosetron level alprazolam: Increased plasma alprazolam level fluvoxamine maleate 458 antihistamines: Increased risk of impaired mental and motor skills aspirin, NSAIDs,
warfarin: Risk of bleeding astemizole, cisapride, pimozide, terfenadine: Possibly fatal QT prolongation benzodiazepines: Decreased benzodiazepine clearance, possibly impaired memory and motor skills buspirone: Decreased buspirone effects, increased blood fluvoxamine level, and paradoxical worsening of obsessive-compulsive disorder carbamazepine: Increased risk of carbamazepine toxicity clozapine: Increased blood clozapine level diltiazem: Increased risk of bradycardia
haloperidol: Increased blood haloperidol level, possibly delayed recall and reduced memory and attention span lithium: Possibly increased serotonin reuptake action of fluvoxamine
MAO inhibitors: Possibly serious or fatal reactions (such as agitation, autonomic instability, coma, delirium, fluctuating vital signs, hyperthermia, myoclonus, and rigidity) methadone: Possibly significantly increased blood methadone level, increased risk of methadone toxicity metoprolol, propranolol: Increased blood levels of these , possibly reduced diastolic blood pressure and heart rate induced by these serotonergics (such as amphetamines and other psychostimulants, antidepressants, and dopamine agonists): Increased risk of serotonin syndrome sympathomimetics: Possibly increased effects of sympathomimetics and increased risk of serotonin syndrome tacrine: Increased blood level and therapeutic and adverse effects of tacrine
theophylline: Decreased theophylline clearance, increased risk of theophylline toxicity tizanidine: Increased risk of serious adverse effects, such as hypotension and profound sedation tricyclic antidepressants: Increased blood levels of antidepressants
warfarin: Increased blood warfarin level, prolonged PT caffeine: Possibly decreased hepatic clearance of caffeine smoking: Increased fluvoxamine metabolism

Side Efect

CNS: Agitation, anxiety, apathy, chills, confusion, depression, dizziness, drowsiness, fatigue, headache, hypomania, insomnia, malaise, mania, nervousness, neuroleptic malignant syndrome, sedation, serotonin syndrome, suicidal ideation, tremor, vertigo, yawning
CV: Palpitations, tachycardia
EENT: Altered taste, blurred vision, dry mouth
GI: Anorexia, constipation, diarrhea, flatulence, indigestion, nausea, upper GI bleeding, vomiting
GU: Decreased libido, ejaculation disorders, impotence, urinary frequency, urine retention
HEME: Bleeding events
MS: Muscle twitching
RESP: Dyspnea, upper respiratory tract infection
SKIN: Diaphoresis, rash
Other: Flulike symptoms, weight gain

Cautions

Use fluvoxamine cautiously in patients with cardiovascular disease, impaired hepatic or renal function, mania, seizures, or suicidal tendencies.
WARNING Fluvoxamine shouldn’t be given within 14 days of an MAO inhibitor.
WARNING Monitor patient for possible serotonin syndrome, characterized by agitation, chills, confusion, diaphoresis, diarrhea, fever, hyperactive reflexes, poor coordination, restlessness, shaking, talking or acting with uncontrolled excitement, tremor, and twitching, especially if patient is receiving another drug that raises serotonin level (such as dopamine agonist, MAO inhibitor, tryptophan, amphetamine, or other antidepressant or psychostimulant). In its most severe form, serotonin syndrome can resemble neuroleptic malignant syndrome, which includes a high fever, muscle rigidity, autonomic instability, and possible fluctuations in vital signs and mental status.

Watch patient closely (especially children, adolescents, and young adults), for suicidal tendencies, particularly when therapy starts and dosage changes, because depresfluvoxamine maleate 459 E F sion may worsen temporarily during these times and lead to suicidal ideation.

Monitor patient for bleeding, especially if patient also takes aspirin, an NSAID, or an anticoagulant. Bleeding can range from ecchymoses, hemtomas, epitaxis, and petechiae to life-threatening hemorrhage.

Discontinue fluvoxamine therapy gradually, as ordered, to prevent unpleasant

Side Efect

.

PATIENT SAFTY

Caution patient not to drink alcohol during fluvoxamine therapy.

Urge patient to avoid potentially hazardous activities until drug’s CNS effects are known.
WARNING Inform patient that fluvoxamine increases the risk of a rare but serious problem: serotonin syndrome. Encourage her to notify prescriber immediately if symptoms develop.

Caution patient not to stop taking drug abruptly. Explain that gradual tapering helps avoid withdrawal symptoms.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes and particularly if patient is a child, teenager, or young adult.

Warn patient that fluvoxamine increases bleeding risk if taken with aspirin, an NSAID, or an anticoagulant and that bleeding events could range from mild to severe. Tell patient to seek emergency care for serious or prlonged bleeding.

Advise pregnant patient to consult with prescriber before her third trimester about ongoing fluvoxamine therapy because of an increased risk to her unborn child during the third trimester.

Category

Chemical class: Water-soluble B-complex vitamin
Therapeutic class: Nutritional supplement Pregnancy category: A

Indications

To prevent deficiency based on U.S. and Canadian recommended daily allowances Adult men and boys age 11 and over. 150 to 400 mcg (150 to 220 mcg Canadian) daily. Adult women and girls age 11 and over. 150 to 400 mcg (145 to 190 mcg Canadian) daily. Pregnant women. 400 to 800 mcg (445 to 475 mcg Canadian) daily. Breast-feeding women. 260 to 800 mcg (245 to 275 mcg Canadian) daily. Children ages 7 to 10. 100 to 400 mcg (125 to 180 mcg Canadian) daily. Children ages 4 to 6. 75 to 400 mcg (90 mcg Canadian) daily. Children from birth to age 3. 25 mcg (50 to 80 mcg Canadian) daily. I.V INFUSION Adults and children age 11 and over. Dosage individualized based on patient need and given as part of total parenteral nutrition solution. To treat folic acid deficiency Adults and children age 11 and over. Dosage individualized based on severity of deficiency, as prescribed.

IV

, I.M. OR SUBCUTANEOUS INJECTION Adults and children age 11 and over. 0.25 to 1 mg daily until hematologic response occurs.

Mechanism of Action

Acts as a catalyst for normal production of red blood cells, helping to prevent megaloblastic anemia, and helps maintain normal homocysteine levels. After being converted to tetrahydrofolic acid in the intestines, folic acid promotes synthesis of several enzymes, including purine and thymidylates; metabolism of amino acids, including glycine and methionine; and metabolism of histidine, all of which are essential for normal cell structure and growth.

Contraindications

Hypersensitivity to folic acid or its components

Interactions

analgesics, carbamazepine, estrogens (including oral contraceptives), phenobarbital, primfolic acid 460 idone: Possibly increased folic acid requirements antacids (aluminumor magnesium-containing), cholestyramine, sulfasalazine: Possibly decreased folic acid absorption hydantoin anticonvulsants: Possibly decreased effectiveness of these , possibly increased folic acid requirements methotrexate, pyrimethamine, triamterene, trimethoprim: Possibly decreased effectiveness of folic acid

Side Efect

Other: Allergic reaction (bronchospasm, erythema, fever, malaise, rash, pruritus)

Cautions

WARNING Don’t give injection form containing benzyl alcohol to neonates or immature infants because a fatal toxic syndrome may occur with CNS, respiratory, circulatory, and renal impairment and metabolic acidosis.

To prevent decreased absorption, give folic acid supplements at least 1 hour before or 4 hours after cholestyramine or sulfasalazine and don’t give antacids within 1 hour before or 2 hours after giving folic acid.

Know that folic acid will correct hematologic disorders in pernicious anemia, but neurologic problems will progressively worsen.

PATIENT SAFTY

Advise against taking folic acid supplements as a substitute for proper dietary intake. Explain that good sources of folic acid include green vegetables, potatoes, cereals, and organ meats. Recommend eating raw green vegetables because heat used during cooking destroys up to 90% of folic acid found in food.

Explain to patients with pernicious anemia that folic acid won’t affect the neurologic symptoms associated with the disease.

Category

Chemical class: Synthetic pentasaccharide factor Xa inhibitor
Therapeutic class: Antithrombolytic

Pregnancy category: B

Indications

To provide prophylaxis against deep vein thrombosis, which may lead to pulmonary embolism in patients undergoing hip fracture surgery, hip replacement surgery, knee replacement surgery, or abdominal surgery in patients at risk for thromboembolic complications SUBCUTANEOUS INJECTION
Adults. Initial: After hemostasis has been established, 2.5 mg subcutaneously 6 to 8 hr after surgery, followed by 2.5 mg subcutaneously daily for 5 to 9 days. Maximum: 2.5 mg subcutaneously daily for 11 days for hip or knee replacement and abdominal surgery and 24 days for hip fracture surgery. To treat acute deep vein thrombosis (with warfarin); to treat acute pulmonary embolism (with warfarin) in a hospital setting SUBCUTANEOUS INJECTION
Adults. Initial: 5 mg if body weight is less than 50 kg (110 lb), 7.5 mg if body weight is 50 to 100 kg (110 to 220 lb), and 10 mg if body weight exceeds 100 kg daily for at least 5 days and until INR is between 2.0 and 3.0 (usually in 5 to 9 days)

Mechanism of Action

Selectively binds to antithrombin III, which enhances the inactivation of clotting factor Xa by antithrombin III. Inactivation of factor Xa interrupts the blood coagulation pathway, which then inhibits thrombin formation. Without thrombin, fibrinogen can’t convert to fibrin and clots can’t form.

Incompatibilities

Don’t mix fondaparinux sodium with other injections or infusions.

Contraindications

Active major bleeding; bacterial endocarditis; body weight less than 50 kg (110 lb) if patient is having hip repair or replacement or knee replacement surgery; fondaparinux-induced thrombocytopenia associated with a positive in vitro test for antiplatelet antibodies; hypersensitivity to fondaparinux; prophylactic fondaparinux therapy in patients weighing less than 50 kg (110 lb) fondaparinux sodium 461 E F undergoing hip repair or replacement, knee replacement, or abdominal surgery; severe renal impairment (creatinine clearance less than 30 ml/min/1.73 m2)

Interactions

abciximab, thrombolytics, other that enhance risk of bleeding: Increased risk of hemorrhage and spinal or epidural hematoma

Side Efect

CNS: Confusion, dizziness, fever, headache, insomnia
CV: Edema, elevated serum aminotransferase level, hypotension
GI: Constipation, diarrhea, elevated liver function test results, indigestion, nausea, vomiting
GU: Urine retention, UTI
HEME: Anemia, bleeding, elevated APTT, hematoma, postoperative hemorrhage, thrombocytopenia, thrombocytopenia with thrombosis
SKIN: Bullous eruption, increased wound drainage, rash, purpura
Other: Generalized pain; hypokalemia; injection site bleeding, pruritus, and rash

Cautions

Fondaparinux shouldn’t be given as prophylaxis for patients who have had a hip fracture, who are having hip or knee replacement or abdominal surgery, or who weigh less than 50 kg (110 lb) because of increased risk of bleeding.

Use fondaparinux cautiously in elderly patients, especially those weighing less than 50 kg (110 lb) and are receiving the drug for pulmomary embolism or deep vein thrombosis, because the risk of druginduced bleeding increases with age.

Don’t give initial dose of fondaparinux less than 6 hours after surgery.

Inspect fondaparinux for particles or discoloration before administration. Be aware that needle guard on prefilled syringe contains dry natural latex rubber and shouldnm’t be handled by those sensitive to latex.

Alternate injection sites using left and right anterolateral or left and right posterolateral abdominal wall. Don’t expel air bubble from prefilled syringe before injection to prevent expelling drug from syringe. Don’t give drug by I.M. injection.
WARNING If patient is receiving fondaparinux with epidural or spinal anesthesia or spinal puncture, watch closely for development of spinal hematoma, which may cause long-term or permanent paralysis. If you see evidence of neurologic impairment, such as changes in sensory or motor function, notify prescriber immediately because urgent care is needed to minimize hematoma’s effect. Risk of spinal or epidural hematoma during fondaparinux therapy is increased by indwelling epidural catheters, concurrent use of other that affect hemostatis, a history of traumatic or repeated epidural or spinal punctures, or a history of spinal deformity or spinal surgery.

Closely monitor patient for bleeding (such as ecchymosis, epistaxis, hematemesis, hematuria, and melena), especially those at risk for decreased drug elimination (such as elderly patients and patients with mild to moderate renal impairment) and those at increased risk for bleeding (such as patients with congenital or acquired bleeding disorders; active ulcerative and angiodysplastic GI disease; hemorrhagic stroke; uncontrolled arterial hypertension; recent brain, spinal, or ophthalmologic surgery; diabetic retinopathy; or a history of heparin-induced thrombocytopenia; and those being treated concomitantly with platelet inhibitors).

Perform periodic CBC, including platelet count, as ordered. Expect prescriber to discontinue drug if platelet count falls below 100,000/mm3. Be aware that routine coagulation tests, such as PT and INR, are not used to monitor fondaparinux therapy; an anti-Xa assay may be used instead. Also, test stools for occult blood, as ordered.

Monitor patient with thrombocytopenia for evidence of thrombosis that may appear similar to heparin-induced thrombocytopenia even when no exposure to heparin has taken place. If patient’s platelet count falls below 100,000/mm3, fondaparinux should be discontinued.

Monitor renal function test results, as ordered. Expect to discontinue drug if severe renal impairment or labile renal function occurs during fondaparinux therapy because the risk of hemorrhage increases as renal function decreases. fondaparinux sodium 462

Store drug at a controlled room temperature.

PATIENT SAFTY

Inform patient that fondaparinux can’t be taken orally.

Instruct patient to seek immediate help if she experiences signs of thromboembolism, such as neurologic changes and severe shortness of breath.

Inform patient about the increased risk of bleeding. Instruct her or family member to watch for and report abdominal or lower back pain, black stools, bleeding gums, bloody urine, or severe headaches.

Teach patient or family member how to administer fondaparinux by subcutaneous injection at home, if needed. Instruct her not to expel air bubble from a prefilled syringe to avoid expelling some of the drug. Tell her to insert the entire needle into a skinfold held between thumb and forefinger, and remind her to alternate administration sites.

To minimize bruising, caution the patient not to rub the injection site after giving the drug.

Review safe handling and disposal of syringes and needles.

Advise patient to have follow-up appointments and prescribed laboratory tests.

Category

Chemical class: Racemic acid salt
Therapeutic class: Bronchodilator

Pregnancy category: C

Indications

To prevent asthma-induced bronchospasm POWDER FOR ORAL INHALATION Adults and children age 5 and over. 12 mcg every 12 hr through inhaler device. Maximum: 24 mcg daily. To prevent exercise-induced bronchospasm POWDER FOR ORAL INHALATION Adults and adolescents age 12 and over. 12 mcg at least 15 min before exercise every 12 hr p.r.n. Maximum: 24 mcg daily. To provide long-term treatment of bronchospasm in patients with chronic bronchitis and emphysema POWDER FOR ORAL INHALATION
Adults. 12 mcg every 12 hr through inhaler device. Maximum: 24 mcg daily. SOLUTION FOR ORAL INHALATION
Adults.20 mcg b.i.d. by nebulization. Maximum: 40 mcg daily. Route Onset Peak Duration Oral 1–3 min Unknown 12 hr inhalation

Mechanism of Action

Selectively attaches to beta2receptors on bronchial membranes, stimulating the intracellular enzyme adenyl cyclase to convert adenosine triphosphate to cAMP. The resulting increase in the intracellular cAMP level relaxes bronchial smooth-muscle cells, stabilizes mast cells, and inhibits histamine release.

Contraindications

Acute asthma, hypersensitivity to formoterol fumarate or its components

Interactions

adrenergics: Possibly increased sympathetic effects of formoterol
beta blockers: Decreased effects of formoterol, possibly severe bronchospasm corticosteroids, non–potassium-sparing diuretics, xanthine derivatives: Possibly increased hypokalemic effect of formoterol disopyramide, MAO inhibitors, phenothiazines, procainamide, quinidine, tricyclic antidepressants: Possibly prolonged QTc interval, increasing risk of ventricular arrhythmias

Side Efect

CNS: Anxiety, dizziness, fatigue, fever, headache, insomnia, malaise, tremor
CV: Angina, arrhythmias, chest pain, hypertension, hypotension, palpitations, tachycardia
EENT: Dry mouth; laryngeal spasm, irritation, or swelling; hoarseness; pharyngitis; rhinitis and tonsillitis (in children); sinusitis formoterol fumarate dihydrate 463 E F
ENDO: Hyperglycemia
GI: Abdominal pain, gastroenteritis, indigestion (in children); nausea
MS: Back pain, leg cramps, muscle spasms
RESP: Asthma exacerbation, bronchitis, bronchospasm (paradoxical or hypersensitivity-induced), cough, dyspnea, increased sputum production, upper respiratory tract infection
SKIN: Dermatitis, pruritus, rash
Other: Anaphylaxis, angioedema, hypokalemia, metabolic acidosis, viral infection (in children)

Cautions

Administer formoterol capsules or solution only by oral inhalation.

Store capsules and solution in their original packaging, and open immediately before use.

To use delivery system for powder form, place capsule in well of inhaler device. Press and release buttons on side of device to pierce capsule. Have patient inhale rapidly and deeply through mouthpiece; drug is dispersed into airways as patient inhales.

Give inhalation solution only by standard jet nebulizer and air compressor.
WARNING Monitor patient for worsening or deteriorating asthma because drug isn’t rapid-acting and shouldn’t be used as a substitute for corticosteroid therapy.

Watch closely for paradoxical bronchospasm; if this occurs, discontinue formoterol immediately and notify prescriber.

Monitor patients with a history of cardiovascular disorders, especially coronary insufficiency, arrhythmias, or hypertension. Notify prescriber of any significant increases in pulse rate or blood pressure or worsening of chronic conditions because formoterol may produce cardiovascular reactions, including angina, arrhythmias, hypertension or hypotension, palpitations, and tachycardia. Drug may need to be discontinued if such reactions occur.

PATIENT SAFTY

Advise patient, especially if she has significant cardiac history, to inform prescriber of any other she takes before beginning formoterol therapy to prevent harmful drug interactions.

Instruct patient to use manufacturer’s plastic device for inhaling powder form of formoterol, to always use new inhaler that comes with each refill, and not to use a spacer. Tell her never to swallow capsules.

Teach patient how to properly store powdered drug and inhaler. Instruct her to avoid exposing capsules to moisture and to always handle them with dry hands because powder inside capsules must be dry to be inhaled. Also advise her to keep inhaler in a dry place and not to wash it.

Teach patient proper use of powdered formoterol delivery system. Instruct her to remove capsule from blister pack just before use, to place capsule in well of inhaler device, to press and release buttons on side of device to pierce capsule, and then to inhale rapidly and deeply through mouthpiece. Emphasize that she should only inhale, not exhale, into device.

For solution form, teach patient how to use, clean, and store nebulizer equipment. Tell her to leave the vial in its original foil pack until just before use.

Instruct patient who currently uses oral or inhaled corticosteroids to continue using them, as prescribed, even if she feels better after starting formoterol.

Caution patient not to increase formoterol dosage or frequency without consulting prescriber because she may need a rapidacting bronchodilator.

Urge patient to notify prescriber if her symptoms worsen, if formoterol becomes less effective, or if she needs more inhalations of short-acting beta2-agonist than usual. This may indicate that her asthma is worsening.

Instruct patient to notify prescriber immediately if she experiences palpitations, chest pain, rapid heart rate, tremor, or nervousness while taking formoterol because dosage may need to be adjusted.

Category

Chemical class: Phosphonic acid derivative
Therapeutic class: Antibiotic

Pregnancy category: B

fosfomycin tromethamine 464

Indications

To treat uncomplicated UTI (acute cystitis) caused by Enterococcus faecalis or Escherichia coli GRANULES FOR Women age 18 and over.3 g as a single dose mixed with water. Route Onset Peak Duration P.O. 2–3 days 48 hr Unknown

Mechanism of Action

Disrupts the formation of bacterial cell walls by blocking cell wall precursors. Specifically, fosfomycin inactivates enolpyruvyl transferase, which irreversibly blocks the condensation of uridine diphosphate-N-acetylglucosamine with phosphoenolpyruvate, a preliminary step in bacterial cell wall synthesis. Fosfomycin also decreases adherence of bacteria to epithelial cells of the urinary tract.

Contraindications

Hypersensitivity to fosfomycin or its components

Interactions

metoclopramide: Decreased blood level and urinary excretion of fosfomycin

Side Efect

CNS: Asthenia, dizziness, fever, headache, insomnia, nervousness, paresthesia, somnolence
EENT: Dry mouth, pharyngitis, rhinitis
GI: Abdominal pain, anorexia, constipation, diarrhea, flatulence, indigestion, nausea, pseudomembranous colitis, vomiting
GU: Dysmenorrhea, dysuria, hematuria, menstrual irregularities, vaginitis
MS: Back pain
SKIN: Pruritus, rash
Other: Flulike symptoms, lymphadenopathy

Cautions

Use fosfomycin cautiously in patients with impaired renal function because drug clearance may be decreased.

Expect to obtain urine specimens for culture and sensitivity tests before and after fosfomycin therapy.

To reconstitute granules, pour contents of single-dose packet into 90 to 120 ml (3 to 4 oz) of water (not hot water) and stir. Administer immediately after dissolving.
WARNING Expect

Side Efect

to increase if more than one dose is used to treat a single episode of acute cystitis.

Monitor patient for diarrhea during and for at least 2 months after drug therapy; diarrhea may signal pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold fosfomycin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

PATIENT SAFTY

Explain how to reconstitute fosfomycin, and instruct patient to take drug immediately after it dissolves. Tell her not to take dry granules or mix them with hot water.

To treat each episode of acute cystitis, advise patient to use only a single dose, as prescribed, to avoid increasing the risk of

Side Efect

.

Urge patient to notify prescriber if symptoms don’t improve in 2 to 3 days.

Instruct patient to return to prescriber for further urine testing after taking fosfomycin.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Explain that watery or bloody stools can occur 2 or more months after therapy and can be serious, requiring prompt treatment.

Category

Chemical class: Phosphinic acid derivative
Therapeutic class: Antihypertensive, vasodilator

Pregnancy category: C

(first trimester), D (later trimesters)

Indications

To manage blood pressure, alone or with other antihypertensives
Adults. Initial: 10 mg daily. Maintenance: 20 to 40 mg daily. Maximum: 80 mg daily. To treat heart failure
Adults.10 mg daily. fosinopril sodium 465 E F
DOSAGE ADJUSTMENT Initial dosage reduced to 5 mg daily, if needed, for patients with acute heart failure, moderate to severe renal failure, or recent aggressive diuresis. Dosage may be increased over several weeks to maximum of 40 mg daily. Route Onset Peak Duration P.O. 1 hr 2–6 hr 24 hr

Mechanism of Action

May reduce blood pressure by affecting renin-angiotensin-aldosterone system. By inhibiting angiotensin-converting enzyme, fosinopril:

prevents conversion of angiotensin I to angiotensin II, a potent vasoconstrictor that also stimulates the adrenal cortex to secrete aldosterone

may inhibit renal and vascular production of angiotensin II

decreases serum angiotensin II level and increases serum renin activity, which decreases aldosterone secretion, slightly increasing the serum potassium level and fluid loss

decreases vascular tone and blood pressure

inhibits aldosterone release, which reduces sodium and water reabsorption and increases their excretion, further reducing blood pressure.

Contraindications

Hypersensitivity to fosinopril, other ACE inhibitors, or their components

Interactions

allopurinol, bone marrow depressants, procainaminde, systemic corticosteroids: Increased risk of potentially fatal neutropenia or agranulocytosis antacids: Impaired fosinopril absorption cyclosporine, potassium-sparing diuretics, potassium supplements: Increased risk of hyperkalemia diuretics, other antihypertensives: Possibly additive hypotension lithium: Increased blood lithium level and risk of lithium toxicity
NSAIDs: Possibly decreased antihypertensive effect of fosinopril sodium aurothiomalate: Nitritoid reactions, including facial flushing, nausea, vomiting, and hypotension salt substitutes: Increased risk of hyperkalemia
alcohol use: Possibly additive hypotension

Side Efect

CNS: Confusion, depression, dizziness, drowsiness, fatigue, fever, headache, insomnia, mood changes, sleep disturbance, syncope, tremor, vertigo, weakness
CV: Angina, arrhythmias (including AV conduction disorders, bradycardia, and tachycardia), claudication, hypotension, MI, orthostatic hypotension, palpitations
EENT: Dry mouth, epistaxis, eye irritation, hoarseness, rhinitis, sinus problems, taste perversion, tinnitus, vision changes
GI: Abdominal distention and pain, anorexia, constipation, diarrhea, flatulence, hepatic failure, hepatitis, hepatomegaly, nausea, pancreatitis, vomiting
GU: Decreased libido, flank pain, renal insufficiency, sexual dysfunction, urinary frequency
MS: Arthralgia, gout, myalgia
RESP: Asthma; bronchitis; bronchospasm; dry, persistent, tickling cough; dyspnea; tracheobronchitis; upper respiratory tract infection
SKIN: Diaphoresis, jaundice, photosensitivity, pruritus, rash, urticaria
Other: Anaphylaxis, angioedema, hyperkalemia, weight gain

Cautions

Monitor serum potassium level before and during fosinopril therapy, as appropriate.

Observe patient being treated for heart failure for at least 2 hours after giving drug to detect hypotension or orthostatic hypotension. If either develops, notify prescriber and monitor patient until blood pressure stabilizes. Keep in mind that orthostatic hypotension is unlikely to develop in patients with a systolic blood pressure over 100 mm Hg who receive a 10-mg dose.

If patient also receives an antacid, separate administration times by at least 2 hours.

If patient also receives a diuretic or another antihypertensive, expect to reduce its dosage over 2 to 3 days before starting fosinopril. If blood pressure isn’t controlled with fosinopril alone, other antihypertenfosinopril sodium 466 sive therapy may resume, as prescribed. If so, observe for excessive hypotension.
WARNING If angioedema affects the face, glottis, larynx, limbs, lips, mucous membranes, or tongue, notify prescriber immediately. Expect to discontinue fosinopril and start appropriate therapy at once. If airway obstruction threatens, promptly give 0.3 to 0.5 ml of epinephrine solution 1:1,000 subcutaneously, as prescribed.

PATIENT SAFTY

Instruct patient to take fosinopril at same time each day to improve compliance and maintain drug’s therapeutic effect.

Emphasize the importance of taking fosinopril as prescribed, even if patient feels well. Caution her not to stop taking drug without consulting prescriber.

Explain that drug helps control—but doesn’t cure—hypertension and that patient may need lifelong therapy.
WARNING Urge patient to seek immediate medical attention for difficulty breathing or swallowing, hoarseness, or swelling of the face, lips, tongue, or throat.

Instruct patient to notify prescriber about persistent, severe nausea, vomiting, and diarrhea; resulting dehydration may lead to hypotension.

Advise patient not to take other or use salt substitutes without consulting prescriber.

Encourage patient to keep scheduled appointments with prescriber to monitor blood pressure, blood test results, and effects of therapy.

Caution patient about possible dizziness.

To minimize effects of orthostatic hypotension, advise patient to rise slowly from a lying or sitting position and to dangle legs over bed for several minutes before standing.

Reinforce prescriber’s recommendations for lifestyle changes, such as smoking cessation, stress reduction, dietary improvements, alcohol avoidance, and regular exercise.

If patient is a woman of childbearing age, urge her to use contraception during therapy because drug may harm fetus.

Advise patient to use caution during exercise and hot weather because of the increased risk of dehydration from excessive sweating.

Category

Chemical class: Hydantoin derivative
Therapeutic class: Anticonvulsant

Pregnancy category: D

Indications

To treat status epilepticus
IV:,
I.M.INJECTION Adults and adolescents. Initial: 15 to 20 mg of phenytoin equivalent (PE)/kg I.V. at 100 to 150 PE/min. Maintenance: 4 to 6 mg PE/kg daily I.V. or I.M. in divided doses b.i.d. to q.i.d. Maximum: 30 mg PE/kg as total loading dose. Children. Initial: 15 to 20 mg PE/kg I.V. given at up to 3 mg PE/kg/min. Maintenance: 4 to 6 mg PE/kg daily I.V. or I.M. in divided doses b.i.d. to q.i.d. To prevent or treat seizures during and after neurosurgery
IV:,
I.M.INJECTION Adults and adolescents.Initial: 10 to 20 mg PE/kg I.V., not to exceed 150 mg PE/min. Maintenance: 4 to 6 mg PE/kg daily I.V. or I.M. in divided doses b.i.d. to q.i.d. Maximum: 30 mg PE/kg as total loading dose.

Mechanism of Action

Is converted from fosphenytoin (a prodrug) to phenytoin, which limits the spread of seizure activity and the start of new seizures. Phenytoin does so by regulating voltage-dependent sodium and calcium channels in neurons, inhibiting calcium movement across neuronal membranes, and enhancing the sodium-potassium-adenosine triphosphatase activity in neurons and glial cells. These actions may stem from phenytoin’s ability to slow the recovery rate of inactivated sodium channels.

Contraindications

Hypersensitivity to fosphenytoin, phenytoin, other hydantoins, or their components

Interactions

acetaminophen (long-term use): Increased fosphenytoin sodium 467 E F risk of hepatotoxicity acyclovir: Decreased blood phenytoin level, loss of seizure control alfentanil: Increased clearance and decreased effectiveness of alfentanil amiodarone, fluoxetine: Possibly increased blood phenytoin level and risk of toxicity antacids: Possibly decreased phenytoin effectiveness antineoplastics: Increased phenytoin metabolism
beta blockers: Increased myocardial depression bupropion, clozapine, loxapine, MAO inhibitors, maprotiline, phenothiazines, pimozide,
thioxanthenes: Possibly lowered seizure threshold and decreased therapeutic effects of phenytoin, possibly intensified CNS depressant effects of these calcium: Possibly impaired phenytoin absorption calcium channel blockers: Possibly increased blood phenytoin level carbamazepine: Decreased blood carbamazepine level, possibly increased blood phenytoin level and risk of toxicity chloramphenicol, cimetidine, disulfiram, isoniazid, methylphenidate, metronidazole, phenylbutazone, ranitidine, salicylates, sulfonamides, trimethoprim: Possibly impaired metabolism of these , increased risk of phenytoin toxicity
CNS depressants: Possibly increased CNS depression corticosteroids, cyclosporine, digoxin, disopyramide, doxycycline, furosemide, levodopa, mexiletine,
quinidine: Decreased therapeutic effects of these diazoxide: Possibly decreased therapeutic effects of both dopamine: Possibly sudden hypotension or cardiac arrest after I.V. fosphenytoin administration estrogenand progestin-containing contraceptives: Possibly breakthrough bleeding and decreased contraceptive effectiveness estrogens, progestins: Decreased therapeutic effects, increased blood phenytoin level felbamate: Possibly impaired metabolism and increased blood level of phenytoin fluconazole, itraconazole, ketoconazole, miconazole: Increased blood phenytoin level folic acid: Increased phenytoin metabolism, decreased seizure control
haloperidol: Possibly lowered seizure threshold and decreased therapeutic effects of phenytoin; possibly decreased blood haloperidol level insulin, oral antidiabetic : Possibly increased blood glucose level and decreased therapeutic effects of these lamotrigine: Possibly decreased therapeutic effects of lamotrigine lidocaine: Possibly decreased blood lidocaine level, increased myocardial depression lithium: Increased risk of lithium toxicity methadone: Possibly increased methadone metabolism, leading to withdrawal symptoms molindone: Possibly lowered seizure threshold, impaired absorption, and decreased therapeutic effects of phenytoin omeprazole: Possibly increased blood phenytoin level oral anticoagulants: Possibly impaired metabolism of these and increased risk of phenytoin toxicity; possibly increased anticoagulant effects initially and then decreased effects with prolonged therapy
rifampin: Possibly decreased therapeutic effects of phenytoin streptozocin: Possibly decreased therapeutic effects of streptozocin sucralfate: Possibly decreased phenytoin absorption tricyclic antidepressants: Possibly lowered seizure threshold and decreased therapeutic effects of phenytoin; possibly decreased blood antidepressant level
valproic acid: Decreased blood phenytoin level, increased blood valproic acid level vitamin D analogues: Decreased vitamin D analogue activity xanthines: Possibly inhibited phenytoin absorption and increased clearance of xanthines zaleplon: Increased clearance and decreased effectiveness of zaleplon
alcohol use: Possibly decreased phenytoin effectiveness

Side Efect

CNS: Agitation, amnesia, asthenia, ataxia, cerebral edema, chills, coma, confusion, delusions, depression, dizziness, emotional lability, encephalitis, encephalopathy, extrapyramidal reactions, fever, headache, fosphenytoin sodium 468 hemiplegia, hostility, hypoesthesia, lack of coordination, malaise, meningitis, nervousness, neurosis, paralysis, personality disorder, positive Babinski’s sign, seizures, somnolence, speech disorders, stroke, stupor, subdural hematoma, syncope, transient paresthesia, tremor, vertigo
CV: Atrial flutter, bradycardia, bundlebranch block, cardiac arrest, cardiomegaly, edema, heart failure, hypertension, hypotension, orthostatic hypotension, palpitations, PVCs, shock, tachycardia, thrombophlebitis
EENT: Amblyopia, conjunctivitis, diplopia, dry mouth, earache, epistaxis, eye pain, gingival hyperplasia, hearing loss, hyperacusis, increased salivation, loss of taste, mydriasis, nystagmus, pharyngitis, photophobia, rhinitis, sinusitis, taste perversion, tinnitus, tongue swelling, visual field defects
ENDO: Diabetes insipidus, hyperglycemia, ketosis
GI: Anorexia, constipation, diarrhea, dysphagia, elevated liver function test results, flatulence, gastritis, GI bleeding, hepatic necrosis, hepatitis, ileus, indigestion, nausea, vomiting
GU: Albuminuria, dysuria, incontinence, oliguria, polyuria, renal failure, urine retention, vaginal candidiasis
HEME: Anemia, easy bruising, leukopenia, thrombocytopenia
MS: Arthralgia, back pain, leg cramps, muscle twitching, myalgia, myasthenia, myoclonus, myopathy
RESP: Apnea, asthma, atelectasis, bronchitis, dyspnea, hemoptysis, hyperventilation, hypoxia, increased cough, increased sputum production, pneumonia, pneumothorax
SKIN: Contact dermatitis, diaphoresis, maculopapular or pustular rash, photosensitivity, skin discoloration, skin nodule, Stevens-Johnson syndrome, transient pruritus, urticaria
Other: Cachexia, cryptococcosis, dehydration, facial edema, flulike symptoms, hyperkalemia, hypokalemia, hypophosphatemia, infection, injection site reaction, lymphadenopathy, sepsis

Cautions

Express the dosage, concentration, and infusion rate of fosphenytoin in PE units. Misreading an order or a label could result in massive overdose.

Refrigerate unopened fosphenytoin at 2° to 8° C (36° to 46° F), but don’t freeze.

Dilute drug in D5W or normal saline solution to 1.5 to 25 mg PE/ml.

Inspect parenteral solution before administration. Discard solution that contains particles or is discolored.

Be aware that drug shouldn’t be given I.M. for status epilepticus because I.V. route allows faster onset and peak.

Keep in mind that I.V. fosphenytoin administration doesn’t require use of a filter, as with phenytoin administration.

Don’t give fosphenytoin solution faster than 150 mg PE/minute because of the risk of hypotension. For a 50-kg (110-lb) patient, infusion typically takes 5 to 7 minutes. Fosphenytoin can be given more rapidly than I.V. phenytoin.

Follow loading dose with maintenance dosage of oral or parenteral phenytoin or parenteral fosphenytoin, as prescribed.

As prescribed, give I.V. benzodiazepine (such as lorazepam or diazepam) with fosphenytoin; otherwise, drug’s full antiepileptic effect won’t be immediate.

Monitor ECG, blood pressure, and respiratory function for 10 to 20 minutes after infusion ends.

Expect to obtain blood fosphenytoin (phenytoin) level 2 hours after I.V. infusion or 4 hours after I.M. injection. Therapeutic level generally ranges from 10 to 20 mcg/ml; steady-state may take several days to several weeks to reach.

Be aware that I.V. or I.M. fosphenytoin may be substituted for oral phenytoin sodium at same total daily dose and frequency. If prescribed, give daily amount in two or more divided doses to maintain seizure control.

When switching between phenytoin and fosphenytoin, remember that small differences in phenytoin bioavailability can lead to significant changes in blood phenytoin level and an increased risk of toxicity.

If drug causes transient, infusion-related paresthesia and pruritus, decrease or discontinue infusion, as ordered.

Monitor CBC for thrombocytopenia or leukopenia—signs of hematologic toxicity. Also monitor serum albumin level and results of renal and liver function tests.

Anticipate increased frequency and severifosphenytoin sodium 469 E F ty of

Side Efect

after I.V. administration in patients with hepatic or renal impairment or hypoalbuminemia.

Discontinue drug, as ordered, if signs of hypersensitivity develop: acute hepatotoxicity (hepatic necrosis and hepatitis), fever, lymphadenopathy, and skin reactions during first 2 months of therapy.

Monitor phenytoin level to detect early signs of toxicity, such as diplopia, nausea, severe confusion, slurred speech, and vomiting. Expect to reduce or stop drug.
WARNING Monitor patient for seizures; at toxic levels, phenytoin is excitatory.
WARNING If patient has bradycardia or heart block rhythm, notify prescriber and expect to withhold drug; severe cardiovascular reactions and death have occurred.

Expect to provide vitamin D supplement if patient has inadequate dietary intake and is receiving long-term anticonvulsant treatment.

Document type, onset, and characteristics of seizures and response to treatment.

PATIENT SAFTY

Inform patient that fosphenytoin typically is used for short-term treatment.

Instruct patient to notify prescriber immediately about bothersome symptoms, especially rash and swollen glands.

Because gingival hyperplasia may develop during long-term therapy, emphasize need for good oral hygiene and gum massage.

Urge patient to consume adequate amounts of vitamin D.

Category

Chemical class: Selective 5-hydroxytryptamine1(5-HT1) receptor agonist, triptan
Therapeutic class: Antimigraine agent

Pregnancy category: C

Indications

To treat acute migraine with or without aura
Adults.2.5 mg, repeated in 2 hr if needed. Maximum: 7.5 mg daily.

Mechanism of Action

Binds to 5-HT1Band 5-HT1Dreceptors on extracerebral and intracranial arteries to inhibit excessive dilation of these vessels. This action may decrease carotid arterial blood flow, thus relieving acute migraines. Frovatriptan may also relieve pain by inhibiting the release of proinflammatory neuropeptides and reducing transmission of trigeminal nerve impulses from sensory nerve endings during a migraine attack.

Contraindications

Hypersensitivity to frovatriptan or its components, basilar or hemiplegic migraines, cerebrovascular or peripheral vascular disease, ischemic or vasospastic coronary artery disease (CAD), uncontrolled hypertension, use within 24 hours of other serotonin-receptor agonists or ergotaminecontaining or ergot-type

Interactions

dihydroergotamine mesylate, other ergotamine-containing : Possibly prolonged vasospastic reaction oral contraceptives, propranolol: Possibly increased blood frovatriptan level selective serotonin reuptake inhibitors, such as citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline; serotonin norepinephrine reuptake inhibitors, such as duloxetine, venlafaxine: Increased risk of life-threatening serotonin syndrome

Side Efect

CNS: Anxiety, dizziness, dysesthesia, fatigue, headache, hypoesthesia, insomnia, paresthesia, seizures, serotonin syndrome
CV: Arrhythmias (such as bradycardia and tachycardia), chest pain, coronary artery vasospasm, ECG changes, MI, myocardial ischemia (transient), palpitations, ventricular fibrillation, ventricular tachycardia
EENT: Abnormal vision, dry mouth, indigestion, rhinitis, sinusitis, tinnitus
GI: Abdominal pain, diarrhea, indigestion, vomiting
MS: Skeletal pain
SKIN: Diaphoresis, flushing
Other: Generalized pain

Cautions

Use frovatriptan cautiously in patients frovatriptan succinate 470 with peripheral vascular disease because drug may cause vasospastic reactions, leading to vascular and colonic ischemia with abdominal pain and bloody diarrhea. Assess patient’s peripheral circulation and bowel sounds during frovatriptan therapy.

Don’t give frovatriptan within 24 hours of another 5-HT1receptor agonist, such as sumatriptan or rizatriptan, or of an ergotamine-containing or ergot-type drug, such as dihydroergotamine or methysergide.

Administer tablet with fluids.

Assess patient for headache before administering second dose. Don’t administer more than three 2.5-mg tablets a day.
WARNING Be aware that some patients have had serious adverse cardiac reactions— including fatal ones—after using 5-HT1 receptor agonists. However, these reactions are extremely rare; most were reported in patients with risk factors for CAD.

Assess patient’s cardiovascular status and institute continuous ECG monitoring, as ordered, immediately after drug administration in patients with cardiovascular risk factors because they’re at risk for asymptomatic cardiac ischemia.

Assess patient for arrhythmias, chest pain, and other signs of heart disease in patients with risk factors for CAD. Expect to periodically assess cardiovascular status of patients on long-term therapy.

Be aware that the safety of treating more than four migraine attacks in 30 days (on average) has not been established.

Regularly monitor blood pressure of hypertensive patients during therapy because frovatriptan may produce a transient increase in blood pressure.
WARNING Monitor patient for possible serotonin syndrome, characterized by agitation, chills, confusion, diaphoresis, diarrhea, fever, hyperactive reflexes, poor coordination, restlessness, shaking, talking or acting with uncontrolled excitement, tremor, and twitching, especially if patient is receiving another drug that raises serotonin level (such as selective serotonin reuptake inhibitors or serotonin norepinephrine reuptake inhibitors). In its most severe form, serotonin syndrome can resemble neuroleptic malignant syndrome, which includes a high fever, muscle rigidity, and autonomic instability with possible fluctuations in vital signs and mental status changes.

PATIENT SAFTY

Instruct patient to read and follow manufacturer’s instructions for using frovatriptan to ensure maximum therapeutic results.

Remind patient not to exceed prescribed daily dosage.

Encourage patient to lie down in a dark, quiet room after taking drug to help relieve migraine.

Instruct patient to seek emergency care for chest, jaw, or neck tightness after drug use because drug may cause coronary artery vasospasm.

Urge patient to report palpitations.

Caution patient about possible adverse CNS effects, and advise her to avoid hazardous activities until drug’s CNS effects are known.

Stress need to report any unusual or severe symptoms immediately.

Category

Chemical class: MAO inhibitor, nitrofuran derivative
Therapeutic class: Antibiotic, antiprotozoal

Pregnancy category: C

Indications

To treat bacterial diarrhea and cholera ORAL SUSPENSION, Adults and adolescents. 100 mg every 6 hr for 5 to 7 days. Infants and children age 1 month and over. 1.25 mg/kg every 6 hr for 5 to 7 days. Maximum: 8.8 mg/kg daily. To treat giardiasis ORAL SUSPENSION, Adults and adolescents. 100 mg every 6 hr for 7 to 10 days. Infants and children age 1 month and over.1.25 to 2 mg/kg every 6 hr for 7 to 10 days. Maximum: 8.8 mg/kg daily.

Mechanism of Action

May interfere with several bacterial enzyme systems through DNA strand damage. Furazolidone also prevents the inactivation furazolidone 471 E F of tyramine by GI and hepatic MAO because it is similar in structure and actions to MAO inhibitors.

Contraindications

Age less than 1 month; hypersensitivity to furazolidone, other nitrofurans, or their components

Interactions

levodopa: Increased therapeutic and adverse effects (particularly hypertension) of levodopa meperidine: Possibly agitation, apnea, coma, diaphoresis, fever, and seizures other MAO inhibitors, sedatives, sympathomimetics, tranquilizers, tricyclic antidepressants: Possibly sudden and severe hypertensive crisis selective serotonin reuptake inhibitors: Increased risk of serotonin syndrome and beverages with high content of tyramine or other vasopressor amines: Possibly sudden and severe hypertensive crisis
alcohol use: Possibly disulfiram-like reaction

Side Efect

CNS: Headache, malaise
ENDO: Hypoglycemia
GI: Abdominal pain, diarrhea, nausea, vomiting
GU: Darkened urine
HEME: Hemolytic anemia, leukopenia
Other: Allergic reaction (arthralgia, dyspnea, fever, hypotension, urticaria, vesicular morbilliform rash)

Cautions

Ask patient if she has a history of blood disorders—especially glucose-6-phosphate dehydrogenase (G6PD) deficiency—before giving furazolidone.

As ordered, check G6PD level before giving furazolidone to whites of Mediterranean and Near Eastern origin, Asians, or blacks; G6PD deficiency may worsen drug’s hemolytic effect.

If no response occurs within 7 days, expect to discontinue drug because organism is resistant. Provide therapy with other antibiotics, as prescribed.

If giardiasis symptoms persist, expect to obtain three stool specimens for analysis several days apart, starting 3 to 4 weeks after treatment ends.

PATIENT SAFTY

Instruct patient to take drug at evenly spaced intervals around the clock.

Advise patient to take drug with food if GI distress occurs.

Direct patient to take a missed dose as soon as she remembers, unless it’s nearly time for the next scheduled dose. Caution against double-dosing.

Instruct patient to take furazolidone for the full time prescribed, even if she feels better before finishing the prescription, because stopping too soon could result in reinfection.

Advise patient to store furazolidone between 59° and 86° F (15° and 30° C), protected from moisture and light.

Inform patient that drug may cause dizziness and usually turns urine brown.

Instruct patient to avoid alcohol during therapy and for 4 days afterward.

Give patient a list of products to avoid during furazolidone therapy and for at least 2 weeks afterward, such as and beverages that contain tyramine and other vasopressor amines (for example, ripe cheese, beer, red and white wine, and smoked or pickled meat, poultry, or fish), OTC appetite suppressants, cough and cold medicines, and other , unless prescribed.

Instruct patient to notify prescriber if she experiences difficult breathing, fever, flushing, itching, muscle aches, or rash.

Category

Chemical class: Sulfonamide
Therapeutic class: Antihypertensive, diuretic

Pregnancy category: C

Indications

To reduce edema caused by cirrhosis, heart failure, and renal disease, including nephrotic syndrome furosemide 472

ORALL

,
Adults. 20 to 80 mg as a single dose, increased by 20 to 40 mg every 6 to 8 hr until desired response occurs. Maximum: 600 mg daily. Children.2 mg/kg as a single dose, increased by 1 to 2 mg/kg every 6 to 8 hr until desired response occurs. Maximum: 6 mg/kg/dose.
IV:, I.V.OR
I.M.INJECTION
Adults. 20 to 40 mg as a single dose, increased by 20 mg every 2 hr until desired response occurs. Children.1 mg/kg as a single dose, increased by 1 mg/kg every 2 hr until desired response occurs. Maximum: 6 mg/kg/dose.
DOSAGE ADJUSTMENT Initial single dose limited to 20 mg for elderly patients. To manage mild to moderate hypertension, as adjunct to treat acute pulmonary edema and hypertensive crisis

ORALL

,
Adults.Initial: 40 mg b.i.d., adjusted until desired response occurs. Maximum: 600 mg daily.
IV: OR INJECTION Adults with normal renal function.40 to 80 mg as a single dose over several minutes. Adults with acute renal failure or pulmonary edema. 100 to 200 mg as a single dose over several minutes.
DOSAGE ADJUSTMENT For patients with acute pulmonary edema without hypertensive crisis, dosage reduced to 40 mg followed by 80 mg 1 hr later if therapeutic response doesn’t occur. Route Onset Peak Duration P.O. 20–60 min 1–2 hr 6–8 hr I.V. 5 min In 30 min 2 hr I.M. 30 min Unknown 2 hr

Mechanism of Action

Inhibits sodium and water reabsorption in the loop of Henle and increases urine formation. As the body’s plasma volume decreases, aldosterone production increases, which promotes sodium reabsorption and the loss of potassium and hydrogen ions. Furosemide also increases the excretion of calcium, magnesium, bicarbonate, ammonium, and phosphate. By reducing intracellular and extracellular fluid volume, the drug reduces blood pressure and decreases cardiac output. Over time, cardiac output returns to normal.

Incompatibilities

Don’t mix furosemide (a milky, buffered alkaline solution) with highly acidic solutions.

Contraindications

Anuria unresponsive to furosemide; hypersensitivity to furosemide, sulfonamides, or their components

Interactions

ACE inhibitors: Possibly first-dose hypotension aminoglycosides, cisplatin: Increased risk of ototoxicity amiodarone: Increased risk of arrhythmias from hypokalemia chloral hydrate: Possibly diaphoresis, hot flashes, and hypertension digoxin: Increased risk of digitalis toxicity related to hypokalemia insulin, oral antidiabetic : Increased blood glucose level lithium: Increased risk of lithium toxicity
NSAIDs: Possibly decreased diuresis phenytoin, probenecid: Possibly decreased therapeutic effects of furosemide propranolol: Possibly increased blood propranolol level thiazide diuretics: Possibly profound diuresis and electrolyte imbalances
alcohol use: Possibly increased hypotensive and diuretic effects of furosemide

Side Efect

CNS: Dizziness, fever, headache, paresthesia, restlessness, vertigo, weakness
CV: Orthostatic hypotension, shock, thromboembolism, thrombophlebitis
EENT: Blurred vision, oral irritation, ototoxicity, stomatitis, tinnitus, transient hearing loss (rapid I.V. injection), yellow vision
ENDO: Hyperglycemia
GI: Abdominal cramps, anorexia, constipation, diarrhea, gastric irritation, hepatocellular insufficiency, indigestion, jaundice, nausea, pancreatitis, vomiting
GU: Bladder spasms, glycosuria
HEME: Agranulocytosis (rare), anemia, aplastic anemia (rare), azotemia, hemolytic furosemide 473 E F anemia, leukopenia, thrombocytopenia
MS: Muscle spasms
SKIN: Bullous pemphigoid, erythema multiforme, exfoliative dermatitis, photosensitivity, pruritus, purpura, rash, urticaria
Other: Allergic reaction (interstitial nephritis, necrotizing vasculitis, systemic vasculitis), dehydration, hyperuricemia, hypochloremia, hypokalemia, hyponatremia, hypovolemia

Cautions

WARNING Use furosemide cautiously in patients with advanced hepatic cirrhosis, especially those who also have a history of electrolyte imbalance or hepatic encephalopathy; drug may lead to lethal hepatic coma.

Obtain patient’s weight before and periodically during furosemide therapy to monitor fluid loss.

For once-a-day dosing, give drug in the morning so patient’s sleep won’t be interrupted by increased need to urinate.

Prepare drug for infusion with normal saline solution, lactated Ringer’s solution, or D5W.

Administer drug slowly I.V. over 1 to 2 minutes to prevent ototoxicity.

Expect patient to have periodic hearing tests during prolonged or high-dose I.V. therapy.

Monitor blood pressure and hepatic and renal function as well as BUN, blood glucose, and serum creatinine, electrolyte, and uric acid levels, as appropriate.

Be aware that elderly patients are more susceptible to hypotensive and electrolytealtering effects and thus are at greater risk for shock and thromboembolism.

If patient is at high risk for hypokalemia, give potassium supplements along with furosemide, as prescribed.

Expect to discontinue furosemide at maximum dosage if oliguria persists for more than 24 hours.

Be aware that furosemide may worsen left ventricular hypertrophy and adversely affect glucose tolerance and lipid metabolism.

Notify prescriber if patient experiences hearing loss, vertigo, or ringing, buzzing, or sense of fullness in her ears. Drug may need to be discontinued.

PATIENT SAFTY

Instruct patient to take furosemide at the same time each day to maintain therapeutic effects. Urge her to take it as prescribed, even if she feels well.

Instruct patient to take the last dose of furosemide several hours before bedtime to avoid sleep interruption from diuresis. If patient receives once-daily dosing, advise her to take the dose in the morning to avoid sleep disturbance caused by nocturia.

Advise patient to change position slowly to minimize effects of orthostatic hypotension and to take furosemide with food or milk to reduce GI distress.

Caution patient about drinking alcoholic beverages, standing for prolonged periods, and exercising in hot weather because these actions increase the hypotensive effect of furosemide.

Emphasize the importance of weight and diet control, especially limiting sodium intake.

Unless contraindicated, urge patient to eat more high-potassium and to take a potassium supplement, if prescribed, to prevent hypokalemia.

Instruct patient to keep follow-up appointments with prescriber to monitor progress. Urge her to notify prescriber about persistent, severe nausea, vomiting, and diarrhea because they may cause dehydration.

Inform diabetic patient that furosemide may increase blood glucose level, and advise her to check her blood glucose level frequently.

Category

Chemical class: Cyclohexane-acetic acid derivative
Therapeutic class: Anticonvulsant

Pregnancy category: C

Indications

To manage postherpetic neuralgia ,,
Adults. Initial: 300 mg on day 1, increased to 300 mg b.i.d. on day 2, increased to 300 mg t.i.d. on day 3, and increased gradually thereafter according to pain response, up to 600 mg t.i.d. Maximum: 1,800 mg daily. As adjunct to treat partial seizures ,, Adults and adolescents.Initial: 300 mg t.i.d., increased gradually according to clinical response. Maintenance: 900 to 1,800 mg daily. Maximum: 3,600 mg daily.
DOSAGE ADJUSTMENT If creatinine clearance is 30 to 60 ml/min/1.73 m2, dosage reduced to 300 mg b.i.d.; if it’s 15 to 29 ml/min/ 1.73 m2, to 300 mg daily; and if it’s less than 15 ml/min/1.73 m2, to 300 mg every other day.

Mechanism of Action

Is structurally like gamma-aminobutyric acid (GABA), the main inhibitory neurotransmitter in the brain. Although gabapentin’s exact

Mechanism of Action

is unknown, GABA inhibits the rapid firing of neurons associated with seizures.

Contraindications

Hypersensitivity to gabapentin or its components

Interactions

aluminumand magnesium-containing antacids: Decreased gabapentin bioavailability
CNS depressants: Increased CNS depression
alcohol use: Increased CNS depression

Side Efect

CNS: Agitation, altered proprioception, amnesia, anxiety, apathy, aphasia, asthenia, ataxia, cerebellar dysfunction, chills, CNS tumors, decreased or absent reflexes, delusions, depersonalization, depression, disappearance of aura, dizziness, dream disturbances, dysesthesia, dystonia, emotional lability, euphoria, facial paralysis, fatigue, fever, hallucinations, headache, hemiplegia, hostility, hyperkinesia, hyperreflexia, hypoesthesia, hypotonia, intracranial hemorrhage, lack of coordination, malaise, migraine headache, nervousness, occipital neuralgia, paranoia, paresis, paresthesia, positive Babinski’s sign, psychosis, sedation, seizures, somnolence, stupor, subdural hematoma, suicidal ideation, syncope, tremor, vertigo
CV: Angina, hypertension, hypotension, murmur, palpitations, peripheral edema, peripheral vascular insufficiency, tachycardia, vasodilation
EENT: Abnormal vision, amblyopia, blepharospasm, cataracts, conjunctivitis, diplopia, dry eyes and mouth, earache, epistaxis, eye hemorrhage, eye pain, gingival bleeding, gingivitis, glossitis, hearing loss, hoarseness, increased salivation, inner ear infection, loss of taste, nystagmus, pharyngitis, photophobia, ptosis (bilateral or unilateral), rhinitis, sensation of fullness in ears, stomatitis, taste perversion, tinnitus, tooth discoloration, visual field defects
GI: Abdominal pain, anorexia, constipation, diarrhea, fecal incontinence, flatulence, gastroenteritis, hemorrhoids, hepatitis, hepatomegaly, increased appetite, indigestion, melena, nausea, thirst, vomiting
GU: Acute renal failure, decreased libido, impotence
HEME: Anemia, coagulation defect, decreased WBC count, leukopenia, thrombocytopenia
MS: Arthralgia, arthritis, back pain, bone fractures, dysarthria, joint stiffness or swelling, muscle twitching, myalgia, positive Romberg test, tendinitis
RESP: Apnea, cough, dyspnea, pneumonia, pseudocroup
SKIN: Abrasion, acne, alopecia, cyst, diaG H I G H I phoresis, dry skin, eczema, hirsutism, pruritus, purpura, rash, seborrhea, urticaria
Other: Dehydration, facial edema, lymphadenopathy, viral infection, weight gain or loss

Cautions

As needed, open gabapentin capsules and mix contents with water, fruit juice, applesauce, or pudding before administration.

Administer initial dose at bedtime to minimize

Side Efect

, especially ataxia, dizziness, fatigue, and somnolence.

Give drug at least 2 hours after an antacid.

Don’t exceed 12 hours between doses on a 3-times-a-day schedule.

Be aware that routine monitoring of blood gabapentin level isn’t needed.
WARNING To discontinue drug or switch to an a different anticonvulsant, expect to change gradually over at least 1 week, as prescribed, to avoid loss of seizure control.

Monitor renal function test results, and expect to adjust dosage, if needed.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

PATIENT SAFTY

If patient has trouble swallowing gabapentin capsules, advise him to open them and sprinkle contents in juice or on soft food immediately before use.

Instruct patient not to take drug within 2 hours after taking an antacid.

Urge patient to take a missed dose as soon as he remembers. If the next dose is in less than 2 hours, tell him to wait 1 to 2 hours before taking it and then resume his regular schedule. Caution against doubling the dose.

Caution patient not to stop drug abruptly.

Inform patient about possible ataxia, dizziness, drowsiness, and nystagmus. Advise him to avoid hazardous activities until drug’s CNS effects are known.

To prevent complications from adverse oral reactions (such as gingivitis), encourage patient to use good oral hygiene and to seek routine dental care.

Explain that adverse effects usually are mild to moderate and decline with time.

Urge patient to keep follow-up appointments with prescriber to check progress.

Urge caregivers to watch closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes, and to report concerns immediately.

Urge woman who becomes pregnant while taking gabapentin to enroll in the North American antiepileptic drug pregnancy registry by calling 1-888-233-2334. Explain that this registry is collecting information about the safety of antiepileptic during pregnancy.

Category

Chemical class: Tertiary alkaloid
Therapeutic class: Antidementia agent

Pregnancy category: B

Indications

To treat mild to moderate Alzheimer’stype dementia

ORALL

,
Adults.Initial: 4 mg b.i.d. Dosage increased by 8 mg daily every 4 wk, if tolerated. Maximum: 12 mg b.i.d.
DOSAGE ADJUSTMENT For patients with moderately impaired hepatic or renal function, maximum dosage shouldn’t exceed 16 mg daily.
Adults. Initial: 8 mg daily. Dosage increased by 8 mg daily every 4 wk if tolerated. Maximum: 24 mg daily. Route Onset Peak Duration P.O. Unknown 1 hr Unknown

Mechanism of Action

Reduces acetylcholine metabolism by competitively and reversibly inhibiting the brain enzyme acetylcholinesterase. Acetylcholineproducing neurons degenerate in the brains of patients with Alzheimer’s disease. Inhibition of acetylcholinesterase increases the amount of acetylcholine, which is needed for nerve impulse transmission.

Contraindications

Hypersensitivity to galantamine hydrobromide or its components, severe hepatic or renal impairment (creatinine clearance less galantamine hydrobromide 476 than 9 ml/min/1.73 m2)

Interactions

amitriptyline, fluoxetine, fluvoxamine, quinidine: Possibly decreased galantamine clearance anticholinergics: Possibly interference with cholinesterase activity cholinergic agonists, cholinesterase inhibitors, neuromuscular blockers: Possibly exaggerated effects of these and galantamine
cimetidine: Possibly increased galantamine bioavailability ketoconazole, paroxetine: Increased galantamine bioavailability

Side Efect

CNS: Aggression, asthenia, depression, dizziness, fatigue, fever, headache, insomnia, malaise, somnolence, stroke, suicidal ideation, syncope, tremor
CV: AV block, bradycardia, chest pain, MI, myocardial ischemia
EENT: Rhinitis
GI: Abdominal pain, anorexia, diarrhea, flatulence, GI bleeding, indigestion, nausea, vomiting
GU: Hematuria, incontinence, renal failure or insufficiency, UTI
HEME: Anemia
Other: Dehydration, hypokalemia, weight loss

Cautions

Give galantamine twice daily with morning and evening meals, and ensure adequate fluid intake to prevent GI symptoms.

If therapy is interrupted for several days, expect to restart drug at lowest dose because benefits are lost when it is discontinued.

Monitor patient’s CV status closely because cholinesterase inhibitors like galantamine may have a depressive effect on sinoatrial and AV nodes and may lead to bradycardia and AV block.

Monitor patient for progressive deterioration of mental status because drug is less effective as Alzheimer's disease progresses and intact cholinergic neurons decrease.

PATIENT SAFTY

Instruct patient to take or caregiver to give regular-strength drug with morning and evening meals. Extended-release capsules should be given once in the morning, preferably with food.

Tell patient or caregiver to notify prescriber immediately if therapy stops for several days. Prescriber may restart at lowest dose.

Instruct patient to maintain adequate fluid intake throughout galantamine therapy.

Advise patient not to drive or perform activities requiring alertness, especially during first weeks of treatment, because drug may cause dizziness and drowsiness.

Inform patient and family members that drug isn’t a cure for Alzheimer’s disease.

Category

Chemical class: Fibric acid derivative, phenoxypentanoic acid
Therapeutic class: Antihyperlipidemic

Pregnancy category: C

Indications

As adjunct (with diet) to treat hyperlipidemia types IIb, IV, and V ,
Adults.600 mg before meals b.i.d. Route Onset Peak Duration P.O. 2–5 days 4 wk Unknown

Mechanism of Action

May decrease hepatic triglyceride production by reducing VLDL synthesis, inhibiting peripheral lipolysis, and decreasing hepatic extraction of free fatty acids. Gemfibrozil also may inhibit synthesis and increase clearance of apolipoprotein B, a carrier molecule for VLDL. In addition, it may accelerate turnover and removal of total cholesterol from the liver while increasing cholesterol excretion in the feces. As a result, triglyceride, total cholesterol, and VLDL levels decrease; the HDL level increases; and the LDL level is unaffected.

Contraindications

Concurrent therapy with repaglinide, gallbladder disease, hepatic or severe renal dysgemfibrozil 477 G H I function, hypersensitivity to gemfibrozil or its components

Interactions

chenodiol, ursodiol: Decreased effectiveness of gemfibrozil HMG-CoA reductase inhibitors: Increased risk of rhabdomyolysis and acute renal failure oral anticoagulants: Increased anticoagulation repaglinide: Increased serum repaglinide level and risk of severe hypoglycemia

Side Efect

CNS: Chills, fatigue, headache, hypoesthesia, paresthesia, seizures, somnolence, syncope, vertigo
CV: Vasculitis
EENT: Blurred vision, cataracts, hoarseness, retinal edema, taste perversion
GI: Abdominal or epigastric pain, cholelithiasis, colitis, diarrhea, flatulence, heartburn, hepatoma, nausea, pancreatitis, vomiting
GU: Decreased male fertility, dysuria, impotence
HEME: Anemia, bone marrow hypoplasia, eosinophilia, leukopenia, thrombocytopenia
MS: Arthralgia, back pain, myalgia, myasthenia, myopathy, myositis, rhabdomyolysis, synovitis
RESP: Cough
SKIN: Eczema, jaundice, pruritus, rash
Other: Anaphylaxis, angioedema, increased risk of bacterial and viral infections, lupuslike symptoms, weight loss

Cautions

Monitor serum triglyceride and cholesterol levels, as appropriate.

Periodically review CBC and liver function test results during therapy, as ordered.

If serum triglyceride and cholesterol levels don’t improve within 3 months, expect to switch to a different drug, as prescribed.

PATIENT SAFTY

Instruct patient to take gemfibrozil 30 minutes before breakfast and 30 minutes before dinner.

Advise patient to take a missed dose as soon as he remembers, unless it’s nearly time for the next dose. Caution against doubling the dose.

Stress importance of a low-fat diet, regular exercise, alcohol avoidance, and smoking cessation, as appropriate.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to notify prescriber if he experiences chills; cough; fever; hoarseness; lower back, side, or muscle pain; painful or difficult urination; severe abdominal pain with nausea and vomiting; tiredness; or weakness.

If patient also takes an oral anticoagulant, urge him to report unusual bleeding or bruising; anticoagulant dosage may need to be reduced.

Advise patient to keep scheduled appointments with prescriber to check progress.

Category

Chemical class: Fluoroquinolone
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To treat acute bacterial exacerbation of chronic bronchitis caused by Streptococcus pneumoniae, Haemophilus influenzae, H. parainfluenzae, or Moraxella catarrhalis
Adults. 320 mg daily for 5 days. To treat mild to moderate communityacquired pneumonia caused by S. pneumoniae, H. influenzae, M. catarrhalis, Mycoplasma pneumoniae, Chlamydia pneumoniae, or Klebsiella pneumoniae
Adults. 320 mg daily for 7 days.
DOSAGE ADJUSTMENT Dosage should be decreased to 160 mg daily in patients with creatinine clearance of 40 ml/min/1.73 m2 or less. Route Onset Peak Duration P.O. 0.5–2 hr Unknown Unknown

Mechanism of Action

Inhibits actions of the enzymes DNA gyrase and topoisomerase IV, which are required gemifloxacin mesylate 478 for bacterial growth, thereby causing bacterial cells to die.

Contraindications

Hypersensitivity to gemifloxacin, its components, or other fluroroquinolones

Interactions

aluminum and magnesium antacids, didanosine as chewable or buffered tablets or pediatric powder for oral solution, ferrous sulfate, sucralfate, zinc or other metal cations: Reduced blood gemifloxacin level antipsychotics; class IA antiarrhythmics, such as procainamide and quinidine; class III antiarrhythmics, such as amiodarone and sotalol; erythromycin; tricyclic antidepressants: Possibly prolonged QT interval probenecid: Increased blood gemifloxacin level
warfarin: Possibly enhanced warfarin anticoagulant effects

Side Efect

CNS: Dizziness, fever, headache, syncope, transient ischemic attack
CV: Peripheral edema, prolonged QT interval, supraventricular tachycardia, vasculitis
EENT: Taste perversion
GI: Abdominal pain, acute hepatic necrosis or failure, diarrhea, elevated liver function test results, hepatitis, jaundice, nausea, pseudomembranous colitis, vomiting
GU: Acute renal insufficiency or failure, interstitial nephritis
HEME: Agranulocytosis, aplastic or hemolytic anemia, elevated platelet count, elevated INR, hemorrhage, leukopenia, pancytopenia, thrombocytopenia
MS: Arthralgia, myalgia, tendinitis, tendon rupture
RESP: Allergic pneumonitis
SKIN: Erythema multiforme, exfoliation, facial swelling, photosensitivity, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, serum sickness

Cautions

Review patient’s medical history before giving gemifloxacin, which shouldn’t be used in patient with a history of prolonged QT interval, patient with uncorrected electrolyte disorders, or patient receiving class IA or III antiarrhythmics because of increased risk of prolonged QT interval. Monitor elderly patients closely because they may be more susceptible to prolonged QT interval.

Use cautiously in patients with CNS disorders, such as epilepsy, or in those prone to seizures because other fluroquinolones have caused seizures, increased intracranial pressure, and toxic psychosis. Monitor patient closely; if CNS alterations occur, notify prescriber immediately and expect drug to be discontinued.

Monitor patient closely for hypersensitivity reaction, which may occur as soon as first dose. If patient has such evidence as angioedema, bronchospasm, dyspnea, itching, rash, jaundice, shortness of breath, and urticaria, notify prescriber immediately and expect drug to be discontinued.

Monitor patients prone to tendinitis, such as the elderly, athletes, and those taking corticosteroids, for reports of tendon pain, inflammation, or rupture. If present, notify prescriber. Expect gemifloxacin to be discontinued, patient placed on bedrest with no exercise of affected limb, and diagnostic tests ordered to confirm rupture.

Notify prescriber about severe or prolonged diarrhea; it may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold gemifloxacin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Monitor patients, especially women under age 40 and postmenopausal women receiving hormone replacement therapy, for rash. It may appear days after therapy stars and resolve in 7 days. Notify prescriber immediately if rash occurs because it can be severe in about 10% of patients.

If patient takes warfarin, monitor coagulation status, as ordered, because adding gemifloxacin may increase risk of bleeding.

PATIENT SAFTY

Tell patient to swallow tablet whole and take with a full glass of liquid.

Warn patient not to increase dose because doing so may cause life-threatening cardiac arrhythmias.

Instruct patient to complete entire course of therapy, even if symptoms decrease gemifloxacin mesylate 479 G H I before prescription is finished.

Caution patient to avoid sun exposure as much as possible while taking gemifloxacin. Patient who can’t avoid sun exposure should apply sunscreen and wear a hat, sunglasses, and long sleeves to cover as much skin as possible.

Instruct patient to maintain adequate hydration throughout therapy to keep urine from becoming too concentrated. Tell patient to increase fluid intake if urine darkens or amount voided decreases.

Caution patient to avoid hazardous activities until CNS effects of drug are known.

Instruct patient to seek medical attention and notify prescriber immediately if he has tendon pain, tenderness, or rupture; evidence of hypersensitivity reaction, such as rash, urticaria, difficulty breathing, or facial swelling; or palpitations or fainting spells. The drug may need to be stopped.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Explain that watery or bloody stools can occur 2 or more months after therapy and can be serious, requiring prompt treatment.

Tell patient to consult prescriber before starting any new medications, including OTC products, because gemifloxacin may interact adversely.

Inform patient that magnesium and/or aluminum antacids; products containing iron; multivitamins containing zinc or other metal cations; and didanosine (Videx) chewable or buffered tablets and pediatric powder for oral solution (if prescribed) shouldn’t be taken within 3 hours before or 2 hours after gemifloxacin and that gemifloxacin should be taken at least 2 hours before sucralfate (if prescribed).

Instruct patient to alert prescriber about severe diarrhea, even up to 2 months after gemifloxacin therapy has ended.

Category

Chemical class: Aminoglycoside derived from Micromonospora purpurea
Therapeutic class: Antibiotic

Pregnancy category: D

Indications

To treat serious bacterial infections caused by aerobic gram-negative organisms and some gram-positive organisms, including Citrobacter species, Enterobacter species, Escherichia coli, Klebsiella species, Proteus species, Pseudomonas aeruginosa, Serratia species, Staphylococcus aureus, and many strains of Streptococcus species
IV:,
I.M.INJECTION Adults and adolescents. 1 to 1.7 mg/kg every 8 hr for 7 to 10 days. Children.2 to 2.5 mg/kg every 8 hr for 7 to 10 days. Infants.2.5 mg/kg every 8 to 16 hr for 7 to 10 days. Premature or full-term neonates up to age 1 week.2.5 mg/kg every 12 to 24 hr for 7 to 10 days.

INTRATHECAL

(INTRALUMBAR OR INTRAVENTRICULAR) INJECTION Adults and adolescents. 4 to 8 mg daily. Infants and children age 3 months and over.1 to 2 mg daily. To treat uncomplicated UTI

IV

,
I.M.INJECTION Adults and adolescents weighing more than 60 kg (132 lb). 160 mg once daily or 80 mg every 12 hr. Adults and adolescents weighing less than 60 kg. 3 mg/kg once daily or 1.5 mg/kg every 12 hr.
DOSAGE ADJUSTMENT Supplemental dose of 1 to 1.7 mg/kg (2 to 2.5 mg/kg for children) given by I.M. injection or I.V. infusion after hemodialysis, based on infection severity.

Mechanism of Action

Binds to negatively charged sites on the outer cell membrane of bacteria, thereby disrupting the membrane’s integrity. Gentamicin also binds to bacterial ribosomal subunits and inhibits protein synthesis. Both actions lead to cell death.

Incompatibilities

Don’t administer gentamicin through same I.V. line as other , especially betalactam antibiotics (penicillins and cephalosporins), because substantial mutual inactivation may occur. Give through sepagentamicin sulfate 480 rate sites.

Contraindications

Hypersensitivity or serious toxic reaction to other aminoglycosides, hypersensitivity to gentamicin or its components

Interactions

aminoglycosides (concurrent use of two or more): Decreased bacterial uptake of each drug, increased risk of ototoxicity and nephrotoxicity cephalosporins, enflurane, methoxyflurane, vancomycin: Increased risk of nephrotoxicity loop diuretics: Increased risk of ototoxicity and nephrotoxicity neuromuscular blockers: Prolonged respiratory depression, increased neuromuscular blockade penicillins: Inactivation of gentamicin by certain penicillins, increased risk of nephrotoxicity

Side Efect

CNS: Acute organic mental syndrome, confusion, depression, fever, headache, increased protein in cerebrospinal fluid, lethargy, myasthenia gravis–like syndrome, neurotoxicity (dizziness, hearing loss, tinnitus, vertigo), peripheral neuropathy or encephalopathy (muscle twitching, numbness, seizures, skin tingling), pseudotumor cerebri
CV: Hypertension, hypotension, palpitations
EENT: Blurred vision, increased salivation, laryngeal edema, ototoxicity, stomatitis, vision changes
GI: Anorexia, nausea, splenomegaly, transient hepatomegaly, vomiting
GU: Nephrotoxicity
HEME: Anemia, eosinophilia, granulocytopenia, increased or decreased reticulocyte count, leukopenia, thrombocytopenia
MS: Arthralgia, leg cramps
RESP: Pulmonary fibrosis, respiratory depression
SKIN: Alopecia, generalized burning sensation, pruritus, purpura, rash, urticaria
Other: Anaphylaxis, injection site pain, superinfection, weight loss

Cautions

Before gentamicin therapy begins, expect to obtain a body fluid or tissue specimen for culture and sensitivity testing, as ordered, or check test results, if available.

Drug is best absorbed when given by I.V. route.Blood level is unpredictable after I.M. administration.

For I.V. use, dilute each dose with 50 to 200 ml normal saline solution or D5W to yield no more than 1 mg/ml. Administer slowly over 30 to 60 minutes.

Don’t give gentamicin through same I.V. line as other without first consulting pharmacist.

Expect to adjust dosage based on peak and trough blood drug levels drawn after third maintenance dose, as prescribed.

Don’t give gentamicin by subcutaneous route because it may be painful.

When assisting with intrathecal injection, use only 2 mg/ml of preservative-free preparation.Drug may be injected directly or delivered by implanted reservoir.

Don’t give drug to pregnant patient because it can cause hearing loss in fetus.
WARNING When giving pediatric injectable form of drug, be alert for allergic reactions—including anaphylaxis and possibly life-threatening asthmatic episodes— because drug contains sodium bisulfite.

Assess patient for evidence of other infections because gentamicin may cause overgrowth of nonsusceptible organisms.

Be aware that premature infants, neonates, and elderly patients have an increased risk of nephrotoxicity.

PATIENT SAFTY

Stress importance of completing full course of gentamicin therapy.

Instruct patient to immediately report

Side Efect

, such as hearing loss, to avoid permanent effects.

Category

Chemical class: Sulfonylurea
Therapeutic class: Antidiabetic

Pregnancy category: C

Indications

To control blood glucose level in type 2 diabetes mellitus
Adults. 1 to 2 mg daily with first meal of glimepiride 481 G H I the day. Maintenance: 1 to 4 mg daily, increased by 1 to 2 mg every 1 to 2 wk as needed for blood glucose control. Maximum: 8 mg daily.
DOSAGE ADJUSTMENT Initial dosage reduced to 1 mg daily if needed for patients with renal impairment. As adjunct (with insulin) to control blood glucose level
Adults.8 mg daily with low-dose insulin. Route Onset Peak Duration P.O. 2–3 hr Unknown Over 24 hr

Mechanism of Action

Stimulates insulin release from beta cells in pancreas. Glimepiride also increases peripheral tissue sensitivity to insulin, either by enhancing insulin binding to cellular receptors or by increasing the number of insulin receptors.

Contraindications

Diabetes complicated by pregnancy; diabetic coma; hypersensitivity to glimepiride, sulfonylureas, or their components; ketoacidosis; sole therapy for type 1 diabetes mellitus

Interactions

ACE inhibitors, anabolic steroids, androgens, azole antifungals, bromocriptine, chloramphenicol, clarithromycin, disopyramide, fibric acid derivatives, fluoxetine, guanethidine, H2-receptor antagonists, insulin, magnesium salts, MAO inhibitors, methyldopa, NSAIDs, octreotide, oral anticoagulants, oxyphenbutazone, phenylbutazone, probenecid, quinidine, quinolones, salicylates, sulfonamides, tetracycline, theophylline, tricyclic antidepressants, urinary acidifiers: Increased risk of hypoglycemia asparaginase, calcium channel blockers, cholestyramine, clonidine, corticosteroids, danazol, diazoxide, estrogen, glucagon, hydantoins, isoniazid, lithium, morphine, nicotinic acid, oral contraceptives, phenothiazines, rifabutin, rifampin, sympathomimetics, thiazide diuretics, thyroid , urinary alkalinizers: Increased risk of hyperglycemia
beta blockers: Possibly hyperglycemia or masking of hypoglycemia signs digoxin: Increased risk of digitalis toxicity pentamidine: Initially hypoglycemia and then hyperglycemia if beta cell damage occurs
alcohol use: Altered blood glucose control (usually hypoglycemia)

Side Efect

CNS: Abnormal gait, anxiety, asthenia, chills, depression, dizziness, fatigue, headache, hypertonia, hypoesthesia, insomnia, malaise, migraine headache, nervousness, paresthesia, somnolence, syncope, tremor, vertigo
CV: Arrhythmias, edema, hypertension, vasculitis
EENT: Blurred vision, conjunctivitis, eye pain, pharyngitis, retinal hemorrhage, rhinitis, taste perversion, tinnitus
ENDO: Hypoglycemia
GI: Anorexia, constipation, diarrhea, elevated liver function test results, epigastric discomfort or fullness, flatulence, heartburn, hunger, nausea, proctocolitis, trace blood in stool, vomiting
GU: Darkened urine, decreased libido, dysuria, polyuria
HEME: Agranulocytosis, aplastic anemia, eosinophilia, hemolytic anemia, hepatic porphyria, leukopenia, pancytopenia
MS: Arthralgia, leg cramps, myalgia
RESP: Dyspnea
SKIN: Allergic skin reactions, diaphoresis, eczema, erythema multiforme, exfoliative dermatitis, flushing, jaundice, lichenoid reactions, maculopapular or morbilliform rash, photosensitivity, pruritus, urticaria
Other: Disulfiram-like reaction

Cautions

Monitor fasting blood glucose level to determine response to glimepiride. Expect to check glycosylated hemoglobin level every 3 to 6 months to evaluate long-term blood glucose control.

Arrange for dietary consultation and diabetic teaching, if appropriate. Ask dietitian to discuss amount of alcohol patient can consume without risking hypoglycemia.

Expect to switch patient to insulin therapy, as prescribed, during physical stress, such as infection, surgery, and trauma.
WARNING Expect a higher risk of hypoglycemia when giving glimepiride to a malnourished or debilitated patient or one with renal, hepatic, pituitary, or adrenal glimepiride 482 insufficiency. Also be aware that hypoglycemia may be more difficult to recognize in patients with autonomic neuropathy, the elderly, and patients taking beta blockers or other sympatholytic agents. Monitor blood glucose level closely.

Monitor patient with a history of allergies to other sulfonamide derivatives closely because he may be allergic to glimepiride. If allergic reactions persist or worsen (dyspnea, drop in blood pressure, or shock), expect drug to be discontinued.

PATIENT SAFTY

Instruct patient to take glimepiride just before first meal of the day. Caution him not to skip the meal after taking drug.

Urge patient not to skip doses or increase dosage without consulting prescriber.

Urge patient to report signs of hypoglycemia, such as anxiety, confusion, dizziness, excessive sweating, headache, and nausea.

Encourage patient to carry candy or other simple sugars to treat mild hypoglycemia.

Advise patient to consult prescriber before taking any OTC drug.

Urge patient to carry identification indicating that he has diabetes.

Teach patient how to monitor his blood glucose level.

Teach patient about exercise, diet, signs of hyperglycemia and hypoglycemia, hygiene, foot care, and ways to avoid infection.

Instruct patient to notify prescriber about darkened urine, difficulty controlling his blood glucose level, easy bruising, fever, rash, sore throat, or unusual bleeding.

If photosensitivity is a problem, instruct patient to avoid direct sunlight and to wear sunscreen.

Category

Chemical class: Sulfonylurea
Therapeutic class: Antidiabetic

Pregnancy category: C

Indications

To control blood glucose level in type 2 diabetes mellitus
Adults.Initial: 5 mg daily with breakfast. Dosage increased by 5 mg daily every 3 mo, if needed. Maintenance: 5 to 10 mg daily. Maximum: 20 mg daily.
Adults. Initial: 5 mg 30 min before first meal of day. Dosage adjusted by 2.5 to 5 mg every 2 to 3 days. For daily dose of 15 mg or less, give as a single dose. For dose above 15 mg daily, give in 2 divided doses. Maximum: 40 mg daily. As adjunct to or replacement for insulin therapy in type 2 diabetes mellitus , Adults who need more than 20 units insulin daily. 5 mg daily, while decreasing insulin dosage by one-half. Further insulin reductions are based on clinical response.
DOSAGE ADJUSTMENT Initial dosage reduced to 2.5 mg daily if needed for patients over age 65 and those with hepatic disease. Route Onset Peak Duration P.O. 10–30 30 min– 12–24 hr min 2 hr P.O. () Unknown Unknown 18–24 hr

Mechanism of Action

Stimulates insulin release from beta cells in pancreas. Glipizide also increases peripheral tissue sensitivity to insulin, either by increasing insulin binding to cellular receptors or by increasing number of insulin receptors.

Contraindications

Diabetes complicated by pregnancy; diabetic coma; hypersensitivity to glipizide, sulfonylureas, or their components; ketoacidosis; sole therapy for type 1 diabetes mellitus

Interactions

ACE inhibitors, anabolic steroids, androgens, azole antifungals, bromocriptine, chloramphenicol, disopyramide, fibric acid derivatives, guanethidine, H2-receptor antagonists, insulin, magnesium salts, MAO inhibitors, methyldopa, octreotide, oral anticoagulants, oxyphenbutazone, phenylbutazone, probenecid, quinidine, salicylates, sulfonamides, tetracycline, theophylline, tricyclic antidepressants, urinary acidifiers: Increased risk of hypoglycemia asparaginase, calcium channel blockers, cholestyramine, clonidine, corticosteroids, glipizide 483 G H I danazol, diazoxide, estrogen, glucagon, hydantoins, isoniazid, lithium, morphine, nicotinic acid, oral contraceptives, phenothiazines, rifabutin, rifampin, sympathomimetics, thiazide diuretics, thyroid , urinary alkalinizers: Increased risk of hyperglycemia
beta blockers: Possibly hyperglycemia or masking of hypoglycemia signs digitalis glycosides: Increased risk of digitalis toxicity pentamidine: Initially hypoglycemia and then hyperglycemia if beta cell damage occurs all : Possibly delayed absorption of tablets if taken within 30 minutes of meal
alcohol use: Altered blood glucose control (usually hypoglycemia)

Side Efect

CNS: Abnormal gait, anxiety, asthenia, chills, depression, dizziness, fatigue, headache, hypertonia, hypoesthesia, insomnia, malaise, migraine headache, nervousness, paresthesia, somnolence, syncope, tremor, vertigo
CV: Arrhythmias, edema, hypertension, vasculitis
EENT: Blurred vision, conjunctivitis, eye pain, pharyngitis, retinal hemorrhage, rhinitis, taste perversion, tinnitus
ENDO: Hypoglycemia
GI: Abdominal pain, anorexia, constipation, diarrhea, elevated liver function test results, epigastric discomfort or fullness, flatulence, heartburn, hunger, nausea, proctocolitis, trace blood in stool, vomiting
GU: Darkened urine, decreased libido, dysuria, polyuria
HEME: Agranulocytosis, aplastic anemia, eosinophilia, hemolytic anemia, hepatic porphyria, leukopenia, pancytopenia
MS: Arthralgia, leg cramps, myalgia
RESP: Dyspnea
SKIN: Allergic skin reactions, diaphoresis, eczema, erythema multiforme, exfoliative dermatitis, flushing, jaundice, lichenoid reactions, maculopapular or morbilliform rash, photosensitivity, urticaria
Other: Disulfiram-like reaction

Cautions

Use cautiously in patients with glucose 6phosphate dehydrogenase deficiency because hemolytic anemia may develop. Monitor patient’s CBC closely.

To improve blood glucose control, give drug in divided doses instead of once daily.

Check blood glucose level at least three times daily for a patient switching from insulin to glipizide. Patients who take more than 40 units of insulin daily may need hospitalization during transition.

If patient gradually loses responsiveness to glipizide, expect to give a second antidiabetic to maintain blood glucose control.

Monitor fasting blood glucose level to determine response to drug. Expect to check glycosylated hemoglobin every 3 to 6 months or as ordered to evaluate longterm blood glucose control.

Expect to switch patient to insulin therapy, as prescribed, during physical stress, such as infection, surgery, or trauma.
WARNING Risk of hypoglycemia is higher when giving glipizide to a malnourished or debilitated patient or one with renal, hepatic, pituitary, or adrenal insufficiency.

PATIENT SAFTY

Tell patient to take glipizide 30 minutes before the first meal of the day. Caution him not to skip the meal after taking the drug.

Advise patient not to skip doses or increase the dosage without consulting prescriber.

Urge patient to report evidence of hypoglycemia, such as anxiety, confusion, dizziness, excessive sweating, headache, and nausea.

Encourage patient to carry candy or other simple sugars to treat mild hypoglycemia.

Caution patient to consult prescriber before taking any OTC .

Urge patient to carry identification indicating that he has diabetes.

Teach patient how to monitor his blood glucose level.

Teach patient about exercise, diet, signs of hyperglycemia and hypoglycemia, hygiene, foot care, and ways to avoid infection.

Instruct patient to notify prescriber if he experiences darkened urine, easy bruising, fever, hypoglycemia or hyperglycemia, rash, sore throat, and unusual bleeding.

If photosensitivity is a problem, instruct patient to avoid direct sunlight and to wear sunscreen.

Category

Chemical class: Synthetic hormone
Therapeutic class: Antihypoglycemic, diagnostic aid adjunct

Pregnancy category: B

Indications

To provide emergency treatment of severe hypoglycemia I.V., I.M., OR SUBCUTANEOUS INJECTION Adults and children weighing more than 20 kg (44 lb) or,with GlucaGen,more than 25 kg (55 lb). 1 mg, repeated in 15 min if needed. Children weighing 20 kg or less or,with GlucaGen,25 kg or less. 0.5 mg, or 0.02 to 0.03 mg/kg, repeated in 15 min, if needed. To provide diagnostic assistance by inhibiting bowel peristalsis in radiologic examination of GI tract
I.V.INJECTION
Adults. 0.25 to 2 mg before procedure. Dose, route, and timing vary with segment of GI tract examined and length of procedure. Route Onset Peak Duration I.V. 5–20 Unknown 90 min* min* I.M. 15–26 Unknown 90 min*|| min*§ SubQ 30–45 Unknown 90 min* min*

Mechanism of Action

Increases production of adenylate cyclase, which catalyzes conversion of adenosine triphosphate to cAMP, a process that in turn activates phosphorylase. Phosphorylase promotes breakdown of glycogen to glucose (glycogenolysis) in the liver. As a result, blood glucose level increases and GI smooth muscles relax.

Incompatibilities

Don’t mix glucagon with sodium chloride or solutions that have a pH of 3.0 to 9.5; use with dextrose solutions instead.

Contraindications

Hypersensitivity to glucagon or its components, pheochromocytoma

Interactions

oral anticoagulants: Possibly increased anticoagulant effects

Side Efect

CV: Hypertension, hypotension (with hypersensitivity reaction), tachycardia
GI: Nausea, vomiting
RESP: Bronchospasm, respiratory distress
SKIN: Urticaria

Cautions

Rouse patient as quickly as possible because prolonged hypoglycemia can cause cerebral damage.

For I.V. use, reconstitute 1-mg vial of glucagon with 1 ml of diluent or 10-mg vial with 10 ml of diluent. Don’t give more than 1 mg/ml. For large doses, dilute with sterile water for injection.

Before injecting glucagon, place unconscious patient on his side to prevent aspiration of vomitus when he regains consciousness.

Administer by slow I.V. injection to decrease risk of

Side Efect

, such as tachycardia and vomiting.

If patient doesn’t respond to glucagon, expect to give I.V. dextrose.

When patient is conscious or diagnostic procedure is completed, give oral carbohydrates to restore hepatic glycogen stores and prevent secondary hypoglycemia.

Keep in mind that glucagon isn’t effective in patients with depleted hepatic glycogen stores caused by such conditions as adrenal insufficiency, chronic hypoglycemia, and starvation.

PATIENT SAFTY

Instruct patient to monitor blood glucose level, especially with signs of hypoglycemia. glucagon 485 G H I * For antihypoglycemic action. 45 sec to 1 min for smooth-muscle relaxation. 9 to 25 min for smooth-muscle relaxation. §4 to 10 min for smooth-muscle relaxation. ||12 to 32 min for smooth-muscle relaxation.

Teach patient and family members how to recognize signs of hypoglycemia and when to notify prescriber.

Advise patient to carry candy or other simple sugars to treat early hypoglycemia.

Emphasize importance of a consistent diet, regular exercise, and proper use of insulin or oral antidiabetic drug.

Make sure unstable diabetic patients and family members know how to give glucagon subcutaneously in case of hypoglycemia. Instruct family members to keep patient on his side and give him a carbohydrate when he awakens. Advise against giving fluids by mouth until patient is fully conscious.

Instruct patient and family members to call for emergency medical assistance after glucagon treatment, especially if patient can’t ingest oral glucose or if he’s taking the sulfonylurea chlorpropamide, in case secondary hypoglycemia occurs.

Category

Chemical class: Sulfonylurea
Therapeutic class: Antidiabetic

Pregnancy category: C

(B for Glynase PresTab and Micronase)

Indications

To control blood glucose level in type 2 diabetes mellitus MICRONIZED
Adults. Initial: 1.5 to 3 mg daily with first meal of day, increased by up to 1.5 mg at weekly intervals, if needed. Maintenance: 0.75 to 12 mg as a single dose or in divided doses with meals. NONMICRONIZED
Adults. Initial: 2.5 to 5 mg daily with first meal of the day, increased by up to 2.5 mg at weekly intervals, if needed. Maintenance: 1.25 to 20 mg daily as a single dose or in divided doses with meals.
DOSAGE ADJUSTMENT For conversion from insulin to glyburide for adults who use more than 40 units of insulin daily, initial dosage adjusted to 5 mg nonmicronized or 3 mg micronized glyburide as a single dose with 50% of usual insulin dose; glyburide dosage increased gradually, as needed. For adults who use less than 40 units insulin daily, usual glyburide dosage is used when insulin is discontinued. For elderly patients, initial dosage possibly reduced to 1.25 mg nonmicronized glyburide daily, gradually increased by 2.5 mg/ wk, as needed; or 0.75 to 3 mg micronized daily, gradually increased by 1.5 mg/wk, as needed. Route Onset Peak Duration P.O.* 1 hr 2.3–3.5 hr 12–24 hr P.O. 15–60 min 1–3 hr 24 hr

Mechanism of Action

Stimulates insulin release from beta cells in the pancreas. Glyburide also increases peripheral tissue sensitivity to insulin either by enhancing insulin binding to cellular receptors or by increasing the number of insulin receptors.

Contraindications

Concurrent therapy with bosentan, diabetes complicated by pregnancy; diabetic ketoacidosis; hypersensitivity to glyburide, sulfonylureas, or their components; ketoacidosis; type 1 diabetes mellitus

Interactions

ACE inhibitors, anabolic steroids, androgens, azole antifungals, bromocriptine, chloramphenicol, clarithromycin, disopyramide, fibric acid derivatives, fluoxetine, guanethidine, H2-receptor antagonists, insulin, magnesium salts, MAO inhibitors, methyldopa, NSAIDs, octreotide, oral anticoagulants, oxyphenbutazone, phenylbutazone, probenecid, quinidine, quinolones, salicylates, sulfonamides, tetracycline, theophylline, tricyclic antidepressants, urinary acidifiers: Increased risk of hypoglycemia asparaginase, calcium channel blockers, cholestyramine, clonidine, corticosteroids, glyburide 486 * Micronized. Nonmicronized. danazol, diazoxide, estrogen, glucagon, hydantoins, isoniazid, lithium, morphine, nicotinic acid, oral contraceptives, phenothiazines, rifabutin, rifampin, sympathomimetics, thiazide diuretics, thyroid , urinary alkalinizers: Increased risk of hyperglycemia
beta blockers: Possibly hyperglycemia or masking of hypoglycemia signs bosentan: Increased risk of elevated liver enzymes cyclosporine: Increased cyclosporine plasma level and toxicity digitalis glycosides: Increased risk of digitalis toxicity miconazole (oral): Possibly severe hypoglycemia oral anticoagulants: Possibly potentiated or weakened anticoagulant effects pentamidine: Initial hypoglycemia and then hyperglycemia if beta cell damage occurs
rifampin: Decreased glyburide effectiveness high-fat : Reduced bioavailability of nonmicronized glyburide
alcohol use: Altered blood glucose control (usually hypoglycemia)

Side Efect

CNS: Abnormal gait, anxiety, asthenia, chills, depression, dizziness, fatigue, headache, hypertonia, hypoesthesia, insomnia, malaise, migraine headache, nervousness, paresthesia, somnolence, syncope, tremor, vertigo
CV: Arrhythmias, edema, hypertension, vasculitis
EENT: Blurred vision, conjunctivitis, eye pain, pharyngitis, retinal hemorrhage, rhinitis, taste perversion, tinnitus
ENDO: Hypoglycemia
GI: Anorexia, constipation, cholestatic jaundice, diarrhea, elevated liver function test results, epigastric discomfort or fullness, flatulence, heartburn, hepatic failure, hepatitis, hunger, nausea, proctocolitis, trace blood in stool, vomiting
GU: Decreased libido, dysuria, polyuria
HEME: Agranulocytosis, aplastic anemia, eosinophilia, hemolytic anemia, hepatic porphyria, leukopenia, pancytopenia
MS: Arthralgia, leg cramps, myalgia
RESP: Dyspnea
SKIN: Allergic skin reactions, diaphoresis, eczema, erythema multiforme, exfoliative dermatitis, flushing, jaundice, lichenoid reactions, maculopapular or morbilliform rash, photosensitivity, urticaria
Other: Disulfiram-like reaction

Cautions

Use cautiously in patients with glucose 6phosphate dehydrogenase deficiency because hemolytic anemia may develop. Monitor patient’s CBC closely.

Give glyburide as single dose before first meal of the day. If patient takes more than 10 mg daily or if severe GI distress occurs, give in 2 divided doses before meals.

Monitor fasting blood glucose level to determine patient’s response to glyburide. Expect to check glycosylated hemoglobin every 3 to 6 months or as ordered to evaluate long-term blood glucose control.

When patient switches from insulin to glyburide, check blood glucose level three times daily before meals.

Be aware that micronized tablets aren’t equal to nonmicronized tablets; they contain smaller particles, which affects drug bioavailability.
WARNING Expect a higher risk of hypoglycemia when giving drug to a malnourished or debilitated patient or one with renal, hepatic, pituitary, or adrenal insufficiency. Also be aware that hypoglycemia may be more difficult to recognize in patients with autonomic neuropathy, the elderly, and patients who are taking beta blockers or other sympatholytic agents. Monitor blood glucose level closely.

Monitor patient with history of allergies to other sulfonamide derivatives closely because he may be allergic to glyburide. If allergic reactions persist or worsen (dyspnea, drop in blood pressure, or shock), expect drug to be discontinued.

Administer insulin as needed and prescribed during periods of increased stress, such as infection, surgery, and trauma.

Arrange for diabetic teaching and consultation between patient and dietitian, if appropriate.

PATIENT SAFTY

Instruct patient to take glyburide just before first meal of he day. Caution him not to skip the meal after taking drug.

Advise patient not to take nonmicronized glyburide with a high-fat meal because it may reduce glyburide bioavailability. glyburide 487 G H I

Caution patient to avoid skipping doses, discontinuing glyburide, or taking OTC without first consulting prescriber.

Teach patient how to monitor his blood glucose level and when to notify prescriber about changes.

Urge patient to report signs of hypoglycemia: anxiety, confusion, dizziness, excessive sweating, headache, and nausea.

Suggest that patient carry candy or other simple sugars to treat mild hypoglycemia.

Urge patient to avoid alcohol because it increases the risk of hypoglycemia.

Advise patient to carry identification indicating that he has diabetes.

Teach patient about exercise, diet, signs of hyperglycemia and hypoglycemia, hygiene, foot care, and ways to avoid infection.

Instruct patient to notify prescriber if he experiences easy bruising, fever, hypoglycemia or hyperglycemia, rash, sore throat, and unusual bleeding.

If photosensitivity is a problem, instruct patient to avoid direct sunlight and to wear sunscreen.

Category

Chemical class: Quaternary ammonium compound
Therapeutic class: Antiarrhythmic, anticholinergic, cholinergic adjunct

Pregnancy category: B

Indications

To treat peptic ulcer disease Adults and adolescents.1 to 2 mg b.i.d. or t.i.d. Maximum: 8 mg daily. I.V.OR
I.M.INJECTION Adults and adolescents.0.1 to 0.2 mg every 4 hr, p.r.n. Maximum: 4 doses daily. To reduce gastric acid and respiratory secretions before anesthesia
I.M.INJECTION Adults and adolescents.0.0044 mg/kg 30 to 60 min before anesthesia or when preanesthesia sedative or opioid is given. Children over age 2. 0.0044 to 0.0088 mg/ kg 30 to 60 min before anesthesia or when preanesthesia sedative or opioid is given. To counteract intraoperative and anesthesia-induced arrhythmias
I.V.INJECTION Adults and adolescents. 0.1 mg, repeated every 2 to 3 min, if needed. Children over age 2. 0.0044 mg/kg. Dose repeated every 2 to 3 min, if needed. Maximum: 0.1 mg as a single dose. As cholinergic adjunct in curariform block
I.V.INJECTION Adults and children over age 2. 0.2 mg glycopyrrolate for each 1 mg neostigmine or 5 mg pyridostigmine when given together. Route Onset Peak Duration P.O. 60 min Unknown 8–12 hr I.V. 1 min Unknown 2–3 hr* I.M., 15–30 30–45 2–3 hr* SubQ min min

Mechanism of Action

Inhibits acetylcholine’s action on postganglionic muscarinic receptors throughout the body. Depending on the receptors’ location, glycopyrrolate produces various effects, such as:

reducing the volume and acidity of gastric secretions

controlling excessive bronchial, pharyngeal, and tracheal secretions and dilating the bronchi

inhibiting vagal stimulation of the heart

relaxing smooth muscle in the GI and GU tracts.

Incompatibilities

Don’t mix glycopyrrolate with alkaline or solutions that have a pH over 6.0 because drug stability may be affected. A pH over 6.0 may occur if glycopyrrolate is mixed with dexamethasone sodium phosphate or LR solution. Gas or precipitate may form if glycopyrrolate is mixed in same syringe as chloramphenicol, diazepam, dimenhydrinate, methohexital sodium, pentobarbital sodium, secobarbital sodium, sodium bicarbonate, or thiopental sodium.

Contraindications

Angle-closure glaucoma, asthma, hemorglycopyrrolate 488 * For vagal blocking effect; up to 7 hr for reduction of saliva. rhage with unstable cardiovascular status, hepatic disease, hypersensitivity to anticholinergics, ileus, intestinal atony, myasthenia gravis, obstructive GI or urinary disorders, severe ulcerative colitis, toxic megacolon

Interactions

anticholinergics, antiparkinsonian , phenothiazines, tricyclic antidepressants: Possibly increased anticholinergic effects antidiarrheals (adsorbent): Decreased glycopyrrolate absorption, leading to decreased therapeutic effectiveness antimyasthenics: Possibly reduced intestinal motility atenolol: Possibly potentiated atenolol effects calciumor magnesium-containing antacids, carbonic anhydrase inhibitors, citrates, sodium bicarbonate: Possibly reduced excretion of glycopyrrolate and increased therapeutic and adverse effects cyclopropane: Possibly ventricular arrhythmias digoxin: Possibly potentiated digoxin effects haloperidol, phenothiazines: Possibly decreased effectiveness of these
ketoconazole: Possibly decreased ketoconazole absorption metoclopramide: Possibly antagonized effects of metoclopramide opioids: Possibly severe constipation and urine retention, risk of ileus potassium chloride: Possibly increased severity of potassium chloride–induced gastric lesions

Side Efect

CNS: Confusion, dizziness, drowsiness, headache, insomnia, nervousness, weakness
CV: Bradycardia (low doses), heart block, palpitations, prolonged QT interval, tachycardia (high doses)
EENT: Blurred vision, cycloplegia, dilated pupils, dry mouth, increased intraocular pressure, loss of taste, mydriasis, nasal congestion, photophobia, taste perversion
GI: Abdominal distention, constipation, dysphagia, nausea, vomiting
GU: Impotence, urinary hesitancy, urine retention
RESP: Dyspnea
SKIN: Decreased sweating (heat exhaustion), dry skin, flushing, pruritus, urticaria
Other: Anaphylaxis

Cautions

Use glycopyrrolate cautiously in patients with autonomic neuropathy, hepatic disease, mild to moderate ulcerative colitis, prostatic hypertrophy, or hiatal hernia because drug’s anticholinergic effect can worsen these conditions; gastric ulcer because drug may delay gastric emptying; and renal disease because drug excretion may be altered.

Give tablets 30 to 60 minutes before meals.

As needed and prescribed, give 2-mg dose at bedtime to ensure overnight control of symptoms.

For I.V. use, administer by direct injection without diluting. Or inject into tubing of flowing I.V. solution unless it contains an alkaline drug or sodium bicarbonate.

Closure system contains dry natural rubber that may cause hypersensitivity reaction if handled by or used to inject someone with latex sensitivity.

Use continuous cardiac monitoring, as ordered, to assess patient for arrhythmias during drug administration.
WARNING Check all doses carefully because even a slight overdose can lead to toxicity.

To prevent overheating caused by decreased sweating, adjust the room temperature and make sure patient is well hydrated.

PATIENT SAFTY

Advise patient to take glycopyrrolate tablets 30 to 60 minutes before meals.

Instruct patient to consult prescriber before taking any OTC .

Caution patient about possible drowsiness and dizziness and need to avoid hazardous activities until drug’s effects are known.

Suggest that patient use sugarless hard candy, ice, or saliva substitute to relieve dry mouth.

Instruct patient to avoid exertion and hot environments because he’s prone to heat exhaustion while taking glycopyrrolate.

Urge patient to drink at least 8 glasses of water daily, unless contraindicated.

Tell patient to notify prescriber about abdominal distention, trouble breathing or urinating, eye pain, irregular heartbeat, sensitivity to light, or severe constipation. glycopyrrolate 489 G H I

Advise patient to wear sunglasses in bright light.

Inform male patient that reversible impotence may occur during therapy.

If urinary hesitancy occurs, advise patient to void before taking each dose.

Category

Chemical class: Human IgG1monoclonal antibody
Therapeutic class: Biologic diseasemodifying anti-rheumatic drug (DMARD)

Pregnancy category: B

Indications

To treat moderate to severe active rheumatoid arthritis in combination with methotrexate; to treat active psoriatic arthritis or ankylosing spondylitis with or without methotrexate or other nonbiologic DMARDs SUBCUTANEOUS INJECTION
Adults.50 mg monthly. Route Onset Peak Duration SubQ Unknown 2–6 days Unknown

Mechanism of Action

Binds to a cytokine protein, tumor necrosis factor alpha (TNFa), to block interaction with its receptors, which prevents biological activity of TNFa. Elevated TNFa levels in the blood, synovium, and joints may play an important role in pathophysiology of such inflammatory diseases as rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis. Reduced TNFa activity in these disorders improves signs and symptoms.

Contraindications

Hypersensitivity to golimumab or its components

Interactions

abatacept, anakinra, rituximab: Possibly increased risk of serious infection cytochrome P-450 substrates such as cyclosporine, theophylline,
warfarin: Effects or blood levels of these may change when golimumab therapy starts or stops live vaccines: Increased risk of adverse vaccine effects

Side Efect

CNS: Dizziness, fever, paresthesia
CV: Hypertension
EENT: Nasopharyngitis, oral herpes, pharyngitis, rhinitis, sinusitis
GI: Elevated liver enzyme levels
RESP: Bronchitis, pneumonia, tuberculosis, upper respiratory tract infection
SKIN: Cellulitis, new or worsening psoriasis
Other: Abscess, antibody formation, infections (including invasive fungal infections and reactivation of hepatitis B infection in chronic carriers), influenza, injection site erythema, lupus-like syndrome, malignancies such as lymphoma or leukemia, sepsis

Cautions

Make sure patient has a tuberculin skin test before therapy starts. If skin test is positive, treatment of latent tuberculosis must start before golimumab therapy starts, as prescribed. Also expect antituberculosis therapy to be started if patient has a history of latent or active tuberculosis, if adequate therapy can’t be confirmed, or if patient has a negative test for latent tuberculosis but also has risk factors for tuberculosis.
WARNING If patient has evidence of an active infection when drug is prescribed, golimumab therapy shouldn’t start until infection has been treated. Monitor all patients for infection during therapy, especially those receiving immunosuppressants. If a serious infection, an opportunistic infection, or sepsis develops, expect prescriber to stop drug and start appropriate antimicrobial therapy.

Patients with a history of cancer, except those successfully treated for nonmelanoma skin cancer, should be thoroughly evaluated before golimumab therapy starts because treatment may pose more risks than benefits. Patients with rheumatoid arthritis may have a higher risk than the general population for developing leukemia while taking a TNF blocker such as golimumab.

Use golimumab cautiously in patients with recurrent infection or increased risk of infection, patients who live in regions golimumab 490 where tuberculosis and histoplasmosis are endemic, and patients with a history of hepatitis B infection because drug increases risk of infection.

Use golimumab cautiously in patients with congestive heart failure, demyelinating disorders such as multiple sclerosis, and hematologic cytopenias because these disorders have occurred with use of other TNF blockers.

Be aware that needle cover of syringe contains dry rubber. Don’t handle if you’re allergic to latex.

Take golimumab out of the refrigerator 30 minutes before giving injection to allow time for drug to warm up to room temperature. Never warm drug in any other way. Rotate injection sites.

PATIENT SAFTY

Explain that first injection of golimumab must be administered with a health care professional present.

Teach patient or caregiver how to give golimumab as a subcutaneous injection at home, if applicable. Tell him to let prefilled syringe or autoinjector sit at room temperature outside carton for 30 minutes before injecting. Tell him not to warm drug in any other way and not to remove needle cover or cap while letting golimumab warm up.

Teach patient using autoinjector not to pull the device away from his skin until he hears a first “click”and then a second “click”indicating the injection is finished. It may take up to 15 seconds before second click is heard and, if device is pulled away from the skin before the second click, a full dose may not have been given.

Emphasize need to inject full amount in prefilled syringe to obtain correct 50-mg dose. Instruct patient to discard any drug left in prefilled syringe or autoinjector.

If patient is allergic to latex, explain that needle cover contains natural dry rubber.

Instruct patient or caregiver to use a puncture resistant container to dispose of needles and syringes at home.

Inform patient that drug must be refrigerated (not frozen).

Urge patient to check expiration dates and not to use outdated drug.

Teach patient to rotate injection sites and never to give injection into an area where skin is tender, bruised, red, or hard.

Explain that tuberculosis may occur during golimumab therapy. Instruct him to report persistent cough, wasting or weight loss, and low-grade fever to prescriber.

Teach patient to recognize evidence of infection and bleeding disorders and to tell prescriber if they occur; drug may need to be stopped. Advise patient to avoid people with infections and to have all prescribed laboratory tests performed.

Inform patient that golimumab therapy increases the risk of certain kinds of cancer, especially lymphomas and leukemias. Emphasize the importance of having follow-up visits and reporting unusual or sudden onset of signs or symptoms.

Caution against receiving live-virus vaccines while taking golimumab; doing so may adversely affect the immune system.

Tell patient to report lupus-like signs and symptoms that, although rare, may occur during therapy, such as chest pain that doesn’t go away, shortness of breath, joint pain, or a rash on cheeks or arms that’s sensitive to the sun. Explain that drug may need to be discontinued if these occur.

Advise patient to tell all health care providers about golimumab therapy and to tell prescriber about any OTC , herbal remedies, and vitamin and mineral supplements being taken.

Category

Chemical class: Carbazole
Therapeutic class: Antiemetic

Pregnancy category: B

Indications

To prevent nausea and vomiting caused by chemotherapy

ORALL

, Adults and adolescents.1 mg up to 1 hr before chemotherapy, repeated 12 hr later. Or, 2 mg up to 1 hr before chemotherapy.
IV: Adults and adolescents.10 mcg/kg diluted and infused over 5 min, starting 30 min granisetron hydrochloride 491 G H I before chemotherapy; or 10 mcg/kg undiluted and infused over 30 sec, starting 30 min before chemotherapy. TRANSDERMAL
Adults.3.1 mg/24 hr patch applied to upper outer arm 24 to 48 hr before chemotherapy and worn up to 7 days. Patch removed no sooner than 24 hr after chemotherapy is completed. To prevent nausea and vomiting caused by radiation therapy

ORALL

, Adults and adolescents.2 mg daily given 1 hr before radiation therapy. To prevent or treat postoperative nausea and vomiting
I.V.INJECTION Adults and adolescents. 1 mg given over 30 sec before induction of anesthesia or immediately before reversal anesthesia for prevention. 1 mg administered over 30 sec after surgery for treatment.

Mechanism of Action

Has a high affinity for serotonin receptors along vagal nerve endings in intestines. Because of this affinity, granisetron prevents nausea and vomiting that usually result when serotonin is released by damaged enterochromaffin cells.

Incompatibilities

Don’t mix granisetron in same solution as other .

Contraindications

Hypersensitivity to granisetron or its components

Interactions

that prolong the QT interval: Increased risk of QT-interval prolongation

Side Efect

CNS: Asthenia, chills, CNS stimulation, drowsiness, fever, headache, insomnia, somnolence
CV: Hypertension, prolonged QT interval
EENT: Taste perversion
GI: Abdominal pain, anorexia, constipation, diarrhea, elevated liver function test results, nausea, vomiting
HEME: Anemia, leukopenia, thrombocytopenia
SKIN: Alopecia, reactions at patch application site (pruritus, rash, redness)

Cautions

Use cautiously in patients with arrhythmias or cardiac conduction disorders because granisetron may prolong QT interval. Patients especially at risk include those with cardiac disease or electrolyte abnormalities and those receiving cardiotoxic chemotherapy or therapy with another drug that prolongs QT interval.

For use with chemotherapy, dilute I.V. preparation of granisetron with normal saline solution or D5W to total volume of 20 to 50 ml. Mixture may be stored up to 24 hours. Use only on days when chemotherapy is given.

Apply transdermal patch to patient’s upper outer arm 24 to 48 hours before chemotherapy, and don’t remove it until at least 24 hours after chemotherapy is completed.

PATIENT SAFTY

Inform patient that granisetron is given orally or I.V. before chemotherapy to help prevent nausea.

Instruct patient to take granisetron tablet without food to avoid reducing drug bioavailability.

Advise patient to report constipation, fever, severe diarrhea, or severe headache. Also caution about possible drowsiness.

Advise patient wearing granisetron patch to cover it with clothing if there’s a risk of exposure to sunlight. Tell patient to continue covering application site with clothing for 10 days after removal of patch.

Category

Chemical class: Glyceryl guaiacolate
Therapeutic class: Expectorant

Pregnancy category: C

guaifenesin 492

Indications

To relieve cough, especially when secretions are thick ,, SYRUP, Adults and adolescents.200 to 400 mg every 4 hr. Maximum: 2,400 mg daily. ,, SYRUP Children ages 6 to 12. 100 to 200 mg every 4 hr. Maximum: 1,200 mg daily. To promote productive cough (MUCINEX) Adults and adolescents.600 to 1,200 mg every 12 hr. Maximum: 2,400 mg daily. Route Onset Peak Duration P.O. 30 min Unknown 4–6 hr

Mechanism of Action

Increases fluid and mucus removal from the upper respiratory tract by increasing the volume of secretions and reducing their adhesiveness and surface tension.

Contraindications

Hypersensitivity to guaifenesin

Side Efect

CNS: Dizziness, headache
GI: Nausea and vomiting (with large doses)
SKIN: Rash, urticaria

Cautions

As prescribed and as appropriate, give liquid forms of guaifenesin to children.

Watch for evidence of more serious condition, such as cough that lasts longer than 1 week, fever, persistent headache, and rash.

PATIENT SAFTY

Instruct patient to take each dose with a full glass of water.

Advise patient not to break, crush, or chew tablets but to swallow them whole.

Tell patient to increase fluid intake (unless contraindicated) to help thin secretions.

Advise patient not to take drug longer than 1 week and to notify prescriber about fever, persistent headache, or rash.

Category

Chemical class: Guanidine derivative
Therapeutic class: Antihypertensive

Pregnancy category: B

Indications

To manage hypertension
Adults.5 mg b.i.d., increased to 20 to 75 mg daily in divided doses t.i.d. or q.i.d., if needed.
DOSAGE ADJUSTMENT Initial dosage reduced to 5 mg daily if needed for patients with renal impairment or creatinine clearance of 30 to 60 ml/min/1.73 m2. Then adjusted after at least 7 days. Initial dosage reduced to 5 mg every other day if needed for patients with creatinine clearance less than 30 ml/min/1.73 m2. Then dosage adjusted after at least 2 wk. Route Onset Peak Duration P.O. 30 min–2 hr 4–6 hr 4–14 hr

Mechanism of Action

Exerts antihypertensive effect at peripheral sympathetic nerve endings. Through an uptake mechanism, guanadrel is stored in adrenergic neurons, where it displaces norepinephrine from its storage sites. This action blocks normal release of norepinephrine in response to nerve impulses, which depletes norepinephrine stores in synapses and relaxes vessel walls, thus reducing peripheral resistance and blood pressure.

Contraindications

Heart failure not caused by hypertension, hypersensitivity to guanadrel or its components, MAO inhibitor use within 1 week of guanadrel use, pheochromocytoma

Interactions

alpha blockers, beta blockers, rauwolfia alkaloids: Possibly orthostatic hypotension or bradycardia amphetamines, appetite suppressants, cyclobenzaprine, haloperidol, loxapine, maprotiline, methylphenidate, phenothiazines, thioxanthenes, tricyclic antidepressants: Decreased antihypertensive effect of guanadrel anticholinergics: Possibly decreased inhibition of gastric acid secretion barbiturates, opioids: Possibly increased guanadrel sulfate 493 G H I hypotensive effect
MAO inhibitors: Possibly severe blood pressure increase
NSAIDs: Possibly sodium and water retention and decreased antihypertensive effect of guanadrel sympathomimetics: Possibly reduced antihypertensive effect of guanadrel, leading to hypertension; possibly potentiated effects of sympathomimetics vasodilators: Increased orthostatic hypotension
alcohol use: Increased hypotensive effect

Side Efect

CNS: Confusion, drowsiness, fatigue, headache, light-headedness, paresthesia, sleep disturbance
CV: Chest pain, orthostatic hypotension, palpitations, peripheral edema
EENT: Blurred vision, dry mouth and throat, glossitis
GI: Abdominal cramps or pain, anorexia, constipation, diarrhea, indigestion, nausea, vomiting
GU: Difficult ejaculation, hematuria, impotence, nocturia, urinary frequency or urgency
MS: Arthralgia, back or neck pain, joint inflammation, leg cramps, muscle weakness, myalgia
RESP: Cough, dyspnea
Other: Excessive weight gain or loss

Cautions

Use guanadrel cautiously in patients with asthma because drug may aggravate this condition. Monitor patient for acute dyspnea, wheezing, and other evidence of asthma attack. Notify prescriber immediately if they develop.
WARNING Assess patient for evidence of overdose, such as blurred vision, dizziness, and syncope.

Be aware that elderly patients have a greater risk of dizziness and syncope.

Assess for signs of fluid retention and heart failure, including crackles, a new S3 heart sound, and sudden weight gain.

PATIENT SAFTY

Explain that guanadrel won’t cure high blood pressure but will help control it.

Instruct patient to take drug at the same time each day to improve compliance and blood pressure control.

Caution patient about possible dizziness, light-headedness, and fainting, especially when getting up from a lying or sitting position. Advise him to rise slowly, especially in the morning, and to sit with his feet dangling for 1 to 2 minutes before standing up.

Instruct patient to sit or lie down immediately if he feels dizzy.

To prevent fainting, advise patient to avoid alcohol, standing for long periods, pursuing excessive exercise, and being overly exposed to hot weather.

Instruct patient to check with prescriber before taking OTC during therapy.

Advise patient to follow a low-sodium diet to help reduce blood pressure and prevent fluid retention.

Category

Chemical class: Guanidine derivative
Therapeutic class: Antihypertensive

Pregnancy category: C

Indications

To manage moderate to severe hypertension and renal hypertension
Adults.Initial: 10 to 12.5 mg daily, increased as needed by 10 to 12.5 mg every wk. Maintenance: 25 to 50 mg daily. Some patients may need up to 300 mg daily. Children.0.2 mg/kg daily, increased p.r.n. by 0.2 mg/kg every 7 to 10 days. Maximum: 3 mg/kg every 24 hr.
DOSAGE ADJUSTMENT Initial dosage increased to 25 to 50 mg daily for hospitalized adults because they can be monitored more closely. Then dosage increased by 25 to 50 mg every other day, p.r.n. Route Onset Peak Duration P.O. Unknown 8 hr Unknown

Mechanism of Action

Exerts antihypertensive effect at peripheral guanethidine monosulfate 494 sympathetic nerve endings. Through an uptake mechanism, guanethidine is stored in adrenergic neurons, where it displaces norepinephrine from its storage sites. This action blocks normal release of norepinephrine in response to nerve impulses, which depletes norepinephrine stores in synapses and relaxes vessel walls, reducing peripheral resistance and blood pressure.

Contraindications

Heart failure not caused by hypertension, hypersensitivity to guanethidine or its components, MAO inhibitor use within 1 week of guanethidine use, pheochromocytoma

Interactions

alpha blockers, beta blockers, rauwolfia alkaloids: Possibly orthostatic hypotension or bradycardia amphetamines, appetite suppressants, cyclobenzaprine, haloperidol, loxapine, maprotiline, methylphenidate, phenothiazines, thioxanthenes, tricyclic antidepressants: Decreased antihypertensive effect of guanethidine anticholinergics: Possibly decreased inhibition of gastric acid secretion barbiturates, opioids: Increased hypotensive effect insulin, oral antidiabetic : Possibly increased antidiabetic effect of these
MAO inhibitors: Possibly severe blood pressure increase
NSAIDs: Possibly sodium and water retention and decreased antihypertensive effect of guanethidine sympathomimetics: Possibly reduced antihypertensive effect of guanethidine, leading to hypertension; possibly potentiated effects of sympathomimetics vasodilators: Increased orthostatic hypotension
alcohol use: Increased hypotensive effect

Side Efect

CNS: Depression, dizziness, fatigue, headache, lassitude, paresthesia, syncope
CV: Angina, bradycardia, orthostatic hypotension, palpitations, peripheral edema
EENT: Blurred vision, dry mouth, glossitis, nasal congestion, parotid gland tenderness, ptosis
GI: Anorexia, constipation, diarrhea (severe), indigestion, nausea, vomiting
GU: Ejaculation disorders, elevated BUN level, impotence, nocturia, priapism, urinary frequency
HEME: Anemia, leukopenia, thrombocytopenia
MS: Leg cramps, muscle twitching, myalgia
RESP: Asthma exacerbation, dyspnea
SKIN: Alopecia, dermatitis
Other: Weight gain

Cautions

As prescribed, stop MAO inhibitor therapy at least 1 week before starting guanethidine.

Because guanethidine has cumulative effects, give a small initial dose and increase gradually, as prescribed. When blood pressure is controlled, expect to reduce dosage to lowest effective level.

Watch for orthostatic hypotension, which occurs most often when patient rises in the morning and is exacerbated by hot weather, exercise, and alcohol. Assess supine and standing blood pressures, especially after
DOSAGE ADJUSTMENTs.

Measure daily weight to help detect fluid retention. Also observe for edema and other signs of heart failure. A thiazide diuretic may be prescribed to decrease sodium and fluid retention.

Notify prescriber if severe diarrhea occurs. Drug may need to be discontinued.

Monitor febrile patient for increased hypotension and

Side Efect

because fever decreases drug requirements.

As ordered, stop giving guanethidine 2 weeks before surgery to reduce risk of cardiac arrest during anesthesia.

PATIENT SAFTY

Teach patient how to recognize orthostatic hypotension, and advise changing position slowly. Explain that symptoms are worse in the morning and worsened by exercise, hot weather, alcohol, and hot showers.

Instruct patient to report fainting, frequent dizziness, and severe diarrhea.

Caution patient to avoid alcohol because it may increase risk of orthostatic hypotension.

Instruct patient to weigh himself daily at the same time, on the same scale, and wearing the same amount of clothing. Advise him to report signs of fluid retention, such as reduced urine volume, sudguanethidine monosulfate 495 G H I den weight increase, and limb swelling.

Urge patient to consult prescriber before taking OTC during guanethidine therapy.

If a diabetic patient takes insulin or a sulfonylurea, instruct him to monitor his blood glucose level more frequently to check for hypoglycemia.

Advise patient to follow a low-sodium diet to help reduce blood pressure and prevent fluid retention.

Category

Chemical class: Dichlorobenzine derivative
Therapeutic class: Antihypertensive

Pregnancy category: B

Indications

To manage hypertension, alone or with other antihypertensives
Adults. 1 mg daily at bedtime, increased if needed to 2 mg after 3 to 4 wk. Increased to 3 mg if needed after another 3 to 4 wk. Maintenance: 2 or 3 mg daily.
DOSAGE ADJUSTMENT Twice-daily administration used if blood pressure tends to rise at the end of 24-hr period. To treat attention deficit hyperactivity disorder (ADHD) Adults and children age 6 and over.Initial: 1 mg once daily, increased, as needed, by 1 mg/wk. Maintenance: 1 to 4 mg once daily. Maximum: 4 mg once daily. Route Onset Peak Duration P.O. Unknown* 8–12 hr24 hr

Mechanism of Action

Decreases sympathetic nerve impulse outflow from the vasomotor center of the brain to the heart and blood vessels by stimulating central alpha2-adrenergic receptors. This action reduces peripheral vascular resistance, renovascular resistance, heart rate, and blood pressure. Prolonged guanfacine use may reduce total peripheral vascular resistance, slightly reducing heart rate. Guanfacine also stimulates growth hormone secretion, reduces circulating plasma catecholamine levels, and reduces left ventricular hypertrophy.

Contraindications

Hypersensitivity to guanfacine

Interactions

CNS depressants: Possibly increased CNS depression ketoconazole and other strong CYP3A4/5 inhibitors: Increased plasma guanfacine level and increased risk of bradycardia, hypotension, and sedation NSAIDs, sympathomimetics, tricyclic antidepressants: Possibly decreased antihypertensive effect of guanfacine other antihypertensives: Possibly increased antihypertensive effect, resulting in hypotension rifampin and other CYP3A4 inducers: Decreased plasma guanfacine level and effectiveness
valproic acid: Increased plasma valproic acid level
alcohol use: Possibly increased CNS depression

Side Efect

CNS: Anxiety, asthenia, confusion, depression, dizziness, drowsiness, fatigue, headache, irritability, lethargy, nervousness, sedation, seizures, somnolence, syncope, weakness
CV: Atrioventricular block, bradycardia, chest pain, hypertension, orthostatic hypotension, sinus arrhythmia
EENT: Conjunctivitis, dry mouth
GI: Abdominal pain, constipation, dyspepsia, elevated liver enzyme levels, nausea, vomiting
GU: Decreased libido, enuresis, impotence, urinary frequency
RESP: Asthma
SKIN: Dermatitis, diaphoresis, pallor, pruritus, purpura, rash
Other: Increased weight guanfacine hydrochloride 496 * For single dose; in 1 wk for multiple doses. For single dose; 1 to 3 mo for multiple doses.

Cautions

Use guanfacine cautiously in patients with cerebrovascular disease, chronic renal or hepatic failure, recent MI, or severe coronary insufficiency.

Give drug at bedtime to minimize daytime sedation.
WARNING Expect to stop hypertension treatment by decreasing dosage gradually over 2 to 4 days. Typically, if patient hasn’t taken drug for 2 or more days, he may have withdrawal symptoms, including abdominal cramps, anxiety, chest pain, diaphoresis, headache, increased salivation, insomnia, irregular heart rate and rhythm, nausea, nervousness, restlessness, tremor, and vomiting. For patients being treated for ADHD, expect to taper dosage gradually over 3 to 7 days by no more than 1 mg every 3 to 7 days to prevent rebound hypertension.

If you suspect that patient has drugrelated depression, notify prescriber immediately and expect to discontinue drug.

PATIENT SAFTY

Instruct patient to take guanfacine at bedtime to reduce daytime drowsiness.

Tell patient not to break, crush, or chew extended-release tablets before swallowing.

Caution patient about possible drowsiness, and advise him to avoid hazardous activities until drug’s CNS effects are known.

Urge patient to avoid consuming alcohol and other CNS depressants while taking guanfacine.

Advise patient to report rash.

Inform male patient that guanfacine may cause impotence. Suggest that he discuss impotence with prescriber, if it occurs.

Caution patient not to stop taking drug abruptly because doing so can cause a dangerous rise in blood pressure along with anxiety and nervousness.

Category

Chemical class: Benzodiazepine
Therapeutic class: Antianxiety

Pregnancy category: D

Controlled substance schedule: IV

Indications

To manage anxiety
Adults. 20 to 40 mg t.i.d. or q.i.d. Optimal: 80 to 160 mg daily.
DOSAGE ADJUSTMENT Dosage reduced to 20 mg once or twice daily if needed for debilitated patients. Route Onset Peak Duration P.O. Slow Unknown 6–8 hr

Mechanism of Action

May potentiate the effects of gammaaminobutyric acid (GABA) and other inhibitory neurotransmitters by binding to specific benzodiazepine receptor sites in limbic and cortical areas of the CNS. By binding to these receptor sites, halazepam increases inhibitory effects of GABA and blocks cortical and limbic arousal.

Contraindications

Acute angle-closure glaucoma, hypersensitivity to halazepam or its components, itraconazole or ketoconazole therapy, psychosis

Interactions

antacids: Possibly altered rate of halazepam absorption barbiturates, CNS depressants, opioids: Increased CNS depression, possibly sedation and impaired motor function cimetidine, diltiazem, disulfiram, erythromycin, fluoxetine, fluvoxamine, isoniazid, itraconazole, ketoconazole, metoprolol, nefazodone, oral contraceptives, propoxyphene, propranolol, ranitidine, valproic acid, verapamil: Decreased halazepam clearance, increased blood level, and increased risk of adverse effects clozapine: Possibly respiratory depression digoxin: Increased blood digoxin level and risk of digitalis toxicity levodopa: Decreased antidyskinetic effect neuromuscular blockers: Increased or blocked neuromuscular blockade theophyllines: Decreased sedative effect of halazepam
alcohol use: Increased CNS depression, possibly sedation and impaired motor function smoking: Decreased halazepam effectiveness halazepam 497 G H I

Side Efect

CNS: Agitation, anxiety, ataxia, confusion, depression, dizziness, drowsiness, euphoria, headache, irritability, nervousness, slurred speech, tremor, weakness
CV: Angina, palpitations, sinus tachycardia
EENT: Diplopia, dry mouth, tinnitus
GI: Abdominal cramps or pain, constipation, diarrhea, increased salivation, nausea, vomiting
GU: Decreased libido, dysuria
MS: Arthralgia
SKIN: Pruritus, rash

Cautions

Use halazepam cautiously in patients with impaired hepatic or renal function, seizure disorders, or suicidal tendencies.

Be aware that risk of halazepam addiction and abuse is relatively high.

Monitor renal and liver function test results, as appropriate, during long-term treatment.

Expect to withdraw drug gradually over 2 weeks to avoid withdrawal symptoms, which include anxiety, confusion, insomnia, psychosis, and seizures.

PATIENT SAFTY

Instruct patient to take halazepam exactly as prescribed and not to stop abruptly because withdrawal symptoms may occur.

Caution patient to avoid alcohol and other CNS depressants during therapy. Advise patient to avoid OTC , such as cough and cold remedies, because they may contain CNS depressants.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to report depression, difficulty voiding, double vision, persistent drowsiness, and rash.

Explain that drug’s full effects may not occur for 6 weeks.

Category

Chemical class: Butyrophenone derivative
Therapeutic class: Antidyskinetic, antipsychotic

Pregnancy category: C

(haloperidol decanoate), not rated (haloperidol, haloperidol lactate)

Indications

To treat psychotic disorders

ORALL

, Adults and adolescents.0.5 to 5 mg b.i.d. or t.i.d. Maximum: Usually 100 mg daily. Children ages 3 to 12. 0.05 mg/kg daily in divided doses b.i.d. or t.i.d. Increased by 0.5 mg every 5 to 7 days, if needed. Maximum: 0.15 mg/kg daily. To treat nonpsychotic behavior disorders and Tourette’s syndrome

ORALL

, Adults and adolescents. 0.5 to 5 mg b.i.d. or t.i.d. Maximum: Usually 100 mg daily. Children ages 3 to 12. 0.05 to 0.075 mg/kg daily in divided doses b.i.d. or t.i.d. Increased by 0.5 mg every 5 to 7 days, if needed. Maximum: 0.075 mg/kg daily.
DOSAGE ADJUSTMENT Initial dosage reduced to 0.5 to 2 mg b.i.d. or t.i.d. if needed for elderly or debilitated patients. To treat acute psychotic episodes
I.M.INJECTION Adults and adolescents. Initial: 2 to 5 mg, with subsequent doses up to every 60 min. Or, if symptoms are controlled, dose may be repeated every 4 to 8 hr. Maximum: Usually 100 mg daily. First oral dose may be given 12 to 24 hr after last parenteral dose. To provide long-term antipsychotic therapy for patients who require parenteral therapy LONG-ACTING I.M.(DECANOATE) INJECTION
Adults. Initial: 10 to 15 times the daily oral dose up to 100 mg. Repeated every 4 wk, if needed. Maximum: 300 mg/mo.

Mechanism of Action

May block postsynaptic dopamine receptors in the limbic system and increase brain turnover of dopamine, producing an antipsychotic effect. haloperidol 498

Contraindications

Blood dyscrasias, bone marrow depression, cerebral arteriosclerosis, coma, concurrent use of large amounts of other CNS depressants, coronary artery disease, epilepsy, hepatic dysfunction, hypersensitivity to haloperidol or its components, Parkinson’s disease, severe hypertension or hypotension, severe CNS depression, subcortical brain damage Route Onset Peak Duration I.M.* Unknown 3–4 daysUnknown

Interactions

amphetamines: Possibly decreased stimulant effects of amphetamines and decreased antipsychotic effect of haloperidol anticholinergics, antidyskinetics, antihistamines: Increased anticholinergic effect and risk of decreased antipsychotic effect of haloperidol anticonvulsants: Possibly decreased effectiveness of anticonvulsants and decreased blood haloperidol level bromocriptine: Possibly decreased effectiveness of bromocriptine
bupropion: Lowered seizure threshold, increased risk of major motor seizure
CNS depressants: Increased CNS depression and risk of respiratory depression and hypotension diazoxide: Possibly hypoglycemia dopamine (high-dose therapy): Possibly decreased vasoconstriction ephedrine: Possibly decreased vasopressor effect of ephedrine epinephrine: Possibly severe hypotension and tachycardia fluoxetine: Increased risk of severe and frequent extrapyramidal effects guanadrel, guanethidine: Decreased hypotensive effects of these levodopa, pergolide: Possibly decreased therapeutic effects of these lithium: Increased risk of neurotoxicity MAO inhibitors, maprotiline, tricyclic antidepressants: Increased sedative and anticholinergic effects of these metaraminol: Possibly decreased vasopressor effect of metaraminol methoxamine: Decreased vasopressor effect, shortened duration of methoxamine action methyldopa: Possibly disorientation, slowed or difficult thought processes phenylephrine: Decreased vasopressor response to phenylephrine
alcohol use: Increased CNS depression and risk of respiratory depression and hypotension

Side Efect

CNS: Agitation, anxiety, confusion, drowsiness, dystonia, euphoria, extrapyramidal reactions that may be irreversible (akathisia, pseudoparkinsonism, tardive dyskinesia), hallucinations, headache, insomnia, neuroleptic malignant syndrome, restlessness, slurred speech, tremor, vertigo
CV: Cardiac arrest, hypertension, orthostatic hypotension, QT-interval prolongation, ventricular arrythmias, tachycardia, torsades de pointes
EENT: Blurred vision, dry mouth, increased salivation (all drug forms); stomatitis (oral solution)
ENDO: Breast engorgement, galactorrhea
GI: Constipation, nausea, vomiting
GU: Decreased libido, difficult ejaculation, impotence, menstrual irregularities, urine retention
HEME: Agranulocytosis, anemia, leukocytosis, leukopenia
SKIN: Diaphoresis, photosensitivity, rash
Other: Heatstroke, weight gain

Cautions

Haloperidol shouldn’t be used to treat dementia-related psychosis in the elderly because of an increased mortality risk.

Use haloperidol cautiously in patients with a history of prolonged QT interval, patients with uncorrected electrolyte disturbances, and patients receiving Class IA or III antiarrhythmics because of an increased risk of prolonged QT interval. Monitor elderly patients closely because they may have an increased risk of prolonged QT interval.

Dilute oral solution with a beverage, such as cola or orange, apple, or tomato juice.

Give haloperidol decanoate (long-acting form prepared in sesame oil to produce haloperidol 499 G H I * For haloperidol decanoate and lactate. For haloperidol decanoate only; 30 to 45 min for haloperidol lactate. slow, sustained release) by deep I.M. injection into gluteal muscle using Z-track technique and 21G needle. Don’t give more than 3 ml per site. Expect to reach stable plasma level after third or fourth dose.

If injection solution has a slight yellow discoloration, be aware that this change doesn’t affect potency.

Watch for tardive dyskinesia (potentially irreversible involuntary movements) in patients receiving long-term therapy, especially elderly women who take large doses.

Monitor CBC, especially if patient has a low WBC count or history of druginduced leukopenia or neutropenia, often during the first few months of therapy. If WBC count drops, especially if neutrophil count drops below 1,000/mm3, expect haloperidol to be discontinued. If neutropenia is significant, also monitor patient for fever or other symptoms of infection and provide appropriate treatment, as prescribed.

If extrapyramidal reactions occur during the first few days of treatment, reduce dosage, as prescribed. If symptoms persist, drug may be discontinued. Dystonia also may occur during first few days of treatment, especially in patients receiving higher doses and in males and younger agegroups. Notify prescriber.

Avoid stopping haloperidol abruptly unless severe

Side Efect

occur.

Monitor for signs of neuroleptic malignant syndrome, a rare but possibly fatal disorder linked to antipsychotic . Signs include altered mental status, arrhythmias, fever, and muscle rigidity.
WARNING Sudden death, QT-interval prolongation, and torsades de pointes, although uncommon, may occur in patients receiving haloperidol despite the lack of such predisposing factors as electrolyte imbalance, concurrent therapy with known to prolong the QT interval, underlying cardiac abnormalities, hypothyroidism, and familial long-QT syndrome.

PATIENT SAFTY

Advise patient to take haloperidol exactly as prescribed and not to stop abruptly because withdrawal symptoms may occur.

To prevent oral mucosal irritation, instruct patient to dilute liquid form with juice or cola before taking it.

Caution patient to avoid skin contact with oral solution because it may cause a rash.

Advise patient to take tablets with food or a full glass of milk or water to reduce GI distress.

Instruct patient to consume adequate fluids and to take precautions against heatstroke.

Urge patient not to drink alcohol during therapy.

If sedation occurs, caution patient to avoid driving and other hazardous activities.

Instruct patient to report repetitive movements, tremor, and vision changes.

Category

Chemical class: Glycosaminoglycan
Therapeutic class: Anticoagulant

Pregnancy category: C

Indications

To prevent and treat deep vein thrombosis and pulmonary embolism, to treat peripheral arterial embolism, and to prevent thromboembolism before and after cardioversion of chronic atrial fibrillation
IV: OR INJECTION
Adults.Loading: 35 to 70 units/kg or 5,000 units by injection. Then 20,000 to 40,000 units infused over 24 hr. Children.Loading: 50 units/kg by injection. Then 100 units/kg infused every 4 hr or 20,000 units/m2infused over 24 hr.
I.V.INJECTION
Adults. Initial: 10,000 units. Maintenance: 5,000 to 10,000 units every 4 to 6 hr. Children. Initial: 50 units/kg. Maintenance: 100 units/kg/dose every 4 hr. I.V.OR SUBCUTANEOUS INJECTION
Adults. Loading: 5,000 units I.V. Then 10,000 to 20,000 units subcutaneously. Maintenance: 8,000 to 10,000 units subcutaneously every 8 hr or 15,000 to 20,000 units subcutaneously every 12 hr. heparin 500 To diagnose and treat disseminated intravascular coagulation (DIC)
IV: OR INJECTION
Adults. 50 to 100 units/kg every 4 hr. Drug may be discontinued if no improvement occurs in 4 to 8 hr. Children. 25 to 50 units/kg every 4 hr. Drug may be discontinued if no improvement occurs in 4 to 8 hr. To prevent postoperative thromboembolism SUBCUTANEOUS INJECTION
Adults.5,000 units 2 hr before surgery and then 5,000 units every 8 to 12 hr for 7 days or until patient is fully ambulatory. To prevent clots in patients undergoing open-heart and vascular surgery
IV: OR INJECTION
Adults. 300 units/kg for procedures that last less than 60 min; 400 units/kg for procedures that last longer than 60 min. Minimum: 150 units/kg. Children. 300 units/kg for procedures that last less than 60 min. Then dosage based on coagulation test results. Minimum: 150 units/kg. To maintain heparin lock patency
I.V.INJECTION
Adults. 10 to 100 units/ml heparin flush solution (enough to fill device) after each use of device.
DOSAGE ADJUSTMENT Increased dosage may be needed if patient needs aggressive anticoagulation to treat or prevent life-threatening thromboses, if heparin will be given I.V., and if heparin has been manufactured under the new standard implemented in October, 2009. (The letter “N”appears in the lot number or after the expiration date on heparin products made under the new standard. An exception is Hospira, which identifies its new-standard products using a lot number starting with “82”or higher.) Route Onset Peak Duration I.V. Immediate Minutes Unknown SubQ 20–60 min Unknown Unknown

Mechanism of Action

Binds with antithrombin III, enhancing antithrombin III’s inactivation of the coagulation enzymes thrombin (factor IIa) and factors Xa and XIa. At low doses, heparin inhibits factor Xa and prevents conversion of prothrombin to thrombin. Thrombin is needed for conversion of fibrinogen to fibrin; without fibrin, clots can’t form. At high doses, heparin inactivates thrombin, preventing fibrin formation and existing clot extension.

Incompatibilities

Don’t mix heparin with any other drug unless you have an order to do so and have checked with pharmacist. Heparin is incompatible with many and solutions, especially ones that contain a phosphate buffer, sodium bicarbonate, or sodium oxalate.

Contraindications

Hypersensitivity to heparin or its components; neonates; severe thrombocytopenia; uncontrolled bleeding, except in DIC

Interactions

antihistamines, digoxin, nicotine, tetracyclines: Decreased anticoagulant effect of heparin aspirin, NSAIDs, platelet aggregation inhibitors, sulfinpyrazone: Increased platelet inhibition and risk of bleeding cefamandole, cefoperazone, cefotetan, methimazole, plicamycin, propylthiouracil,
valproic acid: Possibly hypoprothrombinemia and increased risk of bleeding chloroquine, hydroxychloroquine: Possibly thrombocytopenia and increased risk of hemorrhage ethacrynic acid, glucocorticoids, salicylates: Increased risk of bleeding and GI ulceration and hemorrhage nitroglycerin (I.V.): Possibly decreased anticoagulant effect of heparin probenecid: Possibly increased anticoagulant effect of heparin thrombolytics: Increased risk of hemorrhage smoking: Decreased anticoagulant effect

Side Efect

CNS: Chills, dizziness, fever, headache, peripheral neuropathy
CV: Chest pain, thrombosis
EENT: Epistaxis, gingival bleeding, rhinitis
GI: Abdominal distention and pain, hematemesis, melena, nausea, vomiting
GU: Hematuria, hypermenorrhea
HEME: Easy bruising, excessive bleeding heparin 501 G H I from wounds, thrombocytopenia
MS: Back pain, myalgia, osteoporosis
RESP: Dyspnea, wheezing
SKIN: Alopecia, cyanosis, petechiae, pruritus, urticaria
Other: Anaphylaxis; injection site hematoma, irritation, pain, redness, and ulceration

Cautions

Use heparin cautiously in alcoholics; menstruating women; patients over age 60, especially women; and patients with mild hepatic or renal disease or a history of allergies, asthma, or GI ulcer.
WARNING Be aware that the new standard for manufacturing heparin in the U.S. has decreased its I.V. potency by about 10%. When using this route, determine if the heparin has been manufactured under the new standard by looking for the letter “N” in the lot number or after the expiration date (or, if made by Hospira, the number “82”or higher at the start of the lot number). If giving such heparin, be aware that more drug may be required than in the past to achieve desired level of anticoagulation in some patients. The change in potency also may require more frequent or intensive APTT or ACT monitoring. Change in potency doesn’t appear problematic using subcutaneous route.
WARNING Give heparin only by subcutaneous or I.V. route; I.M. use causes hematoma, irritation, and pain.

Avoid injecting any by I.M. route during heparin therapy, to decrease risk of bleeding and hematoma.
WARNING Don’t use heparin sodium injection as a catheter-lock flush because fatal errors have occurred in children when 1-ml heparin sodium injection vials were confused with 1-ml catheter-lock flush vials. Always examine vial labels closely to ensure correct product is being used.

Administer subcutaneous heparin into anterior abdominal wall, above the iliac crest, and 5 cm (20) or more away from the umbilicus. To minimize subcutaneous tissue trauma, lift adipose tissue away from deep tissues; don’t aspirate for blood before injecting drug; don’t move needle while injecting drug; and don’t massage injection site before or after injection.You can apply gentle pressure to the site after withdrawing needle.

Alternate injection sites, and watch for signs of bleeding and hematoma.

To prepare heparin for continuous infusion, invert container at least six times to prevent drug from pooling. Anticipate slight discoloration of prepared solution; this doesn’t indicate a change in potency.

During continuous I.V. therapy, expect to obtain APTT after 8 hours of therapy. Use the arm opposite the infusion site.

For intermittent I.V. therapy, expect to adjust dose based on coagulation test results performed 30 minutes earlier. Therapeutic range is typically 1.5 to 2.5 times the control.

Bleeding is major adverse effect of heparin therapy. Take safety precautions to prevent bleeding, such as having patient use a softbristled toothbrush and an electric razor. Bleeding may occur at any site and also may indicate an underlying problem, such as GI or urinary tract bleeding. Other sites of bleeding that could be fatal and require immediate attention includes adrenal, ovarian, and retroperitoneal hemorrhage.

Monitor blood test results, and observe for signs of bleeding, such as ecchymosis, epistaxis, hematemesis, hematuria, melena, and petechiae. Thrombocytopenia of any degree should be monitored closely. If platelet count drops below 100,000/mm3 or recurrent thrombosis develops, notify prescriber and expect heparin to be discontinued.

Make sure all health care providers know that patient is receiving heparin.

Keep protamine sulfate on hand to use as an antidote for heparin. Be aware that each milligram of protamine sulfate neutralizes 100 units of heparin.

Be aware that prescriber may order oral anticoagulants before discontinuing heparin to avoid increased coagulation caused by heparin withdrawal. Heparin may be discontinued when full therapeutic effect of oral anticoagulant is achieved.

Know that women over age 60 have highest risk of hemorrhage during therapy.

Watch closely if patient is receiving heparin therapy and nitroglycerin I.V. because PTT may decrease and then rebound after nitroglycerin is discontinheparin 502 ued. Monitor PTT closely, and be prepared to adjust heparin dose, as prescribed.
WARNING Delayed-onset, heparin-induced thrombocytopenia may occur several weeks after heparin is discontinued and may progress to heparin-induced thrombocytopenia thrombosis, causing venous and arterial thromboses.

Various heparin products contain the preservative benzyl alcohol, which isn’t recommended for children under age 1 month because it may cause gasping syndrome, which may be fatal.

PATIENT SAFTY

Explain that heparin can’t be taken orally.

Inform patient about increased risk of bleeding; urge her to avoid injuries and to use a soft-bristled toothbrush and an electric razor.

Urge patient to report any abnormal sign or symptom to prescriber, even weeks after heparin has been discontinued, because of the potential for delayed

Side Efect

.

Advise patient to avoid that interact with heparin,such as aspirin and ibuprofen.

Instruct patient and family to watch for and report abdominal or lower back pain, black stools, bleeding gums, bloody urine, excessive menstrual bleeding, nosebleeds, and severe headaches.

Explain that temporary hair loss may occur.

Advise patient to wear or carry appropriate medical identification.

Category

Chemical class: Natural complex glycosaminoglycan sugar
Therapeutic class: Analgesic

Pregnancy category: Not rated

Indications

To relieve osteoarthritic knee pain in patients who respond inadequately to conservative nonpharmacologic therapy and to simple analgesics INTRA-ARTICULAR INJECTION(ORTHOVISC)
Adults. 30 mg/wk for 3 to 4 wk. INTRA-ARTICULAR INJECTION(EUFLEXXA)
Adults. 20 mg/wk for 3 wk.

Mechanism of Action

Relieves pain associated with osteoarthritis by lubricating the joint and absorbing shock when the joint moves. Hyaluronan is a viscoelastic substance normally found in joint tissues and in the fluid that fills joints; it is instilled directly into the joint.

Contraindications

Hypersensitivity to hyaluronan avian, avian-derived products (such as eggs, feathers, or poultry) or any of their components; knee infections; skin diseases affecting the knee area

Side Efect

CNS: Headache
MS: Acute arthritis, arthralgia, back pain, bursitis
Other: Injection site bruising, edema, erythema, pain, pruritus, or rash

Cautions

Prepare patient for removal of joint effusion, if present, before hyaluronan injection.

Assist the trained health care professional who gives intra-articular injections, as needed, making sure that strict aseptic technique is followed during procedure.

Be aware that prefilled syringe is for single use and that contents of syringe should be used immediately after opening.

PATIENT SAFTY

Inform patient that transient knee pain, swelling, or other localized reactions, such as itchiness or bruising, may occur after hyaluronan injection.

Instruct patient to avoid strenuous or weight-bearing activities lasting longer than 1 hour for 48 hours after injection.

Inform patient that she may feel achy after injection but that this discomfort is typically mild and brief.

Advise patient that pain may not be relieved until after third injection.

Category

Chemical class: Phthalazine derivative
Therapeutic class: Antihypertensive, vasodilator

Pregnancy category: C

Indications

To manage essential hypertension, alone or with other antihypertensives
Adults.Initial: 40 mg daily in divided doses b.i.d. or q.i.d. for first 2 to 4 days and then increased to 100 mg daily in divided doses b.i.d. or q.i.d. for remainder of first wk. Maximum: Usually 200 mg daily, but sometimes 300 to 400 mg daily. Children.0.75 mg/kg daily in divided doses b.i.d. or q.i.d. Increased gradually over 3 to 4 wk. Maximum: 7.5 mg/kg or 200 mg daily. To manage severe essential hypertension when drug can’t be taken orally or when need to reduce blood pressure is urgent I.V.OR
I.M.INJECTION
Adults.5 to 40 mg, repeated as needed. Children.1.7 to 3.5 mg/kg daily in divided doses every 4 to 6 hr, as needed. Route Onset Peak Duration P.O. 20–30 min 1–2 hr 2–4 hr I.V. 5–20 min 10–80 min 2–6 hr I.M. 10–30 min 1 hr 2–6 hr

Mechanism of Action

May act in a manner that resembles organic nitrates and sodium nitroprusside, except that hydralazine is selective for arteries. It:

exerts a direct vasodilating effect on vascular smooth muscle

interferes with calcium movement in vascular smooth muscle by altering cellular calcium metabolism

dilates arteries, not veins, which minimizes orthostatic hypotension and increases cardiac output and cerebral blood flow

causes reflex autonomic response that increases heart rate, cardiac output, and left ventricular ejection fraction

has a positive inotropic effect on the heart.

Incompatibilities

Don’t mix hydralazine in I.V. infusion solutions.

Contraindications

Coronary artery disease, hypersensitivity to hydralazine or its components, mitral valve disease

Interactions

beta blockers: Increased effects of both diazoxide, MAO inhibitors, other antihypertensives: Risk of severe hypotension epinephrine: Possibly decreased vasopressor effect of epinephrine
NSAIDs: Decreased hydralazine effects sympathomimetics: Possibly decreased antihypertensive effect of hydralazine all : Possibly increased bioavailability of hydralazine

Side Efect

CNS: Chills, fever, headache, peripheral neuritis
CV: Angina, edema, orthostatic hypotension, palpitations, tachycardia
EENT: Lacrimation, nasal congestion
GI: Anorexia, constipation, diarrhea, nausea, vomiting
RESP: Dyspnea
SKIN: Blisters, flushing, pruritus, rash, urticaria
Other: Lupus-like symptoms, especially with high doses; lymphadenopathy

Cautions

Monitor CBC, lupus erythematosus cell preparation, and ANA titer before therapy and periodically as appropriate during long-term treatment.

Anticipate that drug may change color in solution. Consult pharmacist if color changes.

Be aware that hydralazine may change color when exposed to a metal filter.

Give tablets with food to increase bioavailability.

Monitor blood pressure and pulse rate regularly and weigh patient daily during therapy.

Check blood pressure with patient in lying, sitting, and standing positions, and watch for signs of orthostatic hypotension. Expect orthostatic hypotension to be most common in the morning, during hot weather, and with exercise.
WARNING Expect to discontinue drug immediately if patient has lupus-like hydralazine hydrochloride 504 symptoms, such as arthralgia, fever, myalgia, pharyngitis, and splenomegaly.

Expect prescriber to withdraw hydralazine gradually to avoid a rapid increase in blood pressure.

Expect to treat peripheral neuritis with pyridoxine.

PATIENT SAFTY

Instruct patient to take hydralazine tablets with food.

Advise patient to change position slowly, especially in the morning. Caution that hot showers may increase hypotension.

Instruct patient to immediately notify prescriber about fever, muscle and joint aches, and sore throat.

Urge patient to report numbness and tingling in limbs, which may require treatment with another drug.

Caution patient against stopping drug abruptly because doing so may cause severe hypertension.

Category

Chemical class: Benzothiadiazide
Therapeutic class: Antihypertensive, diuretic

Pregnancy category: B

Indications

To manage hypertension
Adults. 12.5 mg daily.

ORALL

,
Adults.25 to 100 mg daily as a single dose or in divided doses b.i.d. Children age 6 months and over. 1 to 2 mg/kg daily as a single dose or in divided doses b.i.d. Infants under age 6 months.Up to 3 mg/kg daily. As adjunct to treat edema caused by cirrhosis, corticosteroids, estrogen, heart failure, or renal disorders

ORALL

,
Adults.25 to 100 mg b.i.d., once daily, or every other day for 3 to 5 days/wk. Children age 6 months and over.1 to 2 mg/kg daily as a single dose or in divided doses b.i.d. Infants under age 6 months. Up to 3 mg/kg daily. Route Onset Peak Duration P.O. 2 hr 4 hr 6–12 hr

Contraindications

Anuria; hypersensitivity to hydrochlorothiazide, other thiazides, sulfonamide derivatives, or their components; renal failure

Interactions

ACTH, amphotericin B, corticosteroids: Increased electrolyte depletion, especially potassium amantadine: Possibly increased blood level and risk of toxicity of amantadine amiodarone: Increased risk of arrhythmias from hypokalemia antihypertensives: Increased antihypertensive effects barbiturates, opioids: Possibly orthostatic hypotension calcium: Possibly increased serum calcium level cholestyramine, colestipol: Reduced GI absorption of hydrochlorothiazide diazoxide: Increased antihypertensive and hyperglycemic effects of hydrochlorothiazide diflunisal: Possibly increased blood hydrochlorothiazide level digoxin: Increased risk of digitalis toxicity from hypokalemia dopamine: Possibly increased diuretic effects of both insulin, oral antidiabetic : Possibly increased blood glucose level lithium: Decreased lithium clearance, increased risk of lithium toxicity neuromuscular blockers: Possibly enhanced neuromuscular blockade from hypokalemia nondeplarizing skeletal muscle relaxants: Possibly increased response to muscle relaxants
NSAIDs: Decreased diuretic effect of hydrochlorothiazide, increased risk of renal failure oral anticoagulants: Possibly decreased anticoagulant effects sympathomimetics: Possibly decreased antihypertensive effect of hydrochlorothiazide hydrochlorothiazide 505 G H I
vitamin D: Increased risk of hypercalcemia
alcohol use: Possibly orthostatic hypotension

Side Efect

CNS: Dizziness, fever, headache, insomnia, paresthesia, vertigo, weakness
CV: Hypotension, orthostatic hypotension, vasculitis
EENT: Blurred vision, dry mouth
ENDO: Hyperglycemia
GI: Abdominal cramps, anorexia, constipation, diarrhea, indigestion, jaundice, nausea, pancreatitis, vomiting
GU: Decreased libido, impotence, interstitial nephritis, nocturia, polyuria, renal failure
HEME: Agranulocytosis, aplastic anemia, hemolytic anemia, leukopenia, neutropenia, thrombocytopenia
MS: Muscle spasms and weakness
SKIN: Alopecia, cutaneous vasculitis, erythema multiforme, exfoliative dermatitis, photosensitivity, purpura, rash, StevensJohnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, dehydration, hypercalcemia, hyperuricemia, hypochloremia, hypokalemia, hyponatremia, hypovolemia, metabolic alkalosis, weight loss

Cautions

Give hydrochlorothiazide in the morning and early evening to avoid nocturia.

Monitor fluid intake and output, daily weight, blood pressure, and serum levels of electrolytes, especially potassium.

Assess for evidence of hypokalemia, such as muscle spasms and weakness.

Monitor BUN and serum creatinine levels.

Check blood glucose level often, as ordered, in diabetic patients, and expect to increase antidiabetic dosage, as needed.

If patient has gouty arthritis, expect increased risk of gout attacks during therapy.

PATIENT SAFTY

Advise patient to take hydrochlorothiazide morning and early evening to avoid awakening during the night to urinate.

Instruct patient to take drug with food or milk if adverse GI reactions occur.

Tell patient to weigh herself at the same time each day wearing the same amount of clothing and to notify prescriber if she gains more than 2 lb (0.9 kg) per day or 5 lb (2.3 kg) per week.

Instruct patient to eat a diet high in potassium-rich food, including citrus fruits, bananas, tomatoes, and dates.

Advise patient to change position slowly to minimize effects of orthostatic hypotension.

Urge patient to report decreased urination, muscle cramps and weakness, and unusual bleeding or bruising. hydrochlorothiazide 506 Nephron Distal convoluted tubule Peritubular capillary ClNa+ H2O

Mechanism of Action

A thiazide diuretic, hydrochlorothiazide promotes movement of sodium (Na+), chloride (Cl–), and water (H2O) from blood in peritubular capillaries into nephron’s distal convoluted tubule, as shown. Initially, it may decrease extracellular fluid volume, plasma volume, and cardiac output, which helps explain blood pressure reduction. It also may reduce blood pressure by direct arterial dilation.After several weeks, extracellular fluid volume, plasma volume, and cardiac output return to normal, and peripheral vascular resistance remains decreased.

Category

Chemical class: Glucocorticoid
Therapeutic class: Adrenocorticoid replacement, anti-inflammatory

Pregnancy category: Not rated

; C (Cortifoam)

Indications

To treat severe inflammation or acute adrenal insufficiency ORAL SUSPENSION,(HYDROCORTISONE, HYDROCORTISONE CYPIONATE)
Adults.20 to 240 mg daily as a single dose or in divided doses.
IV: OR I.V., I.M., OR SUBCUTANEOUS INJECTION(HYDROCORTISONE SODIUM PHOSPHATE);
I.M.INJECTION(HYDROCORTISONE)
Adults. 15 to 240 mg daily as a single dose or in divided doses. Usual: One-half to onethird the oral dose.
DOSAGE ADJUSTMENT Dosage increased to more than 240 mg daily if needed to treat acute disease.
IV:; I.V.OR
I.M.INJECTION (HYDROCORTISONE SODIUM SUCCINATE)
Adults.100 to 500 mg every 2, 4, or 6 hr. To treat joint and tissue inflammation INTRA-ARTICULAR INJECTION(HYDROCORTISONE ACETATE)
Adults. 25 to 37.5 mg injected into large joints or bursae as a single dose, or 10 to 25 mg into small joints as a single dose. INTRALESIONAL INJECTION(HYDROCORTISONE ACETATE)
Adults. 5 to 12.5 mg injected into tendon sheaths as a single dose, or 12.5 to 25 mg injected into ganglia as a single dose. SOFT-TISSUE INJECTION(HYDROCORTISONE ACETATE)
Adults.25 to 50 mg as a single dose. Sometimes a dose of up to 75 mg is needed. As adjunct to treat ulcerative proctitis of the distal portion of the rectum in patients who can’t retain hydrocortisone or other corticosteroid enemas RECTAL AEROSOL(HYDROCORTISONE ACETATE) Adult men. Initial: 1 applicatorful once or twice daily for 2 to 3 wk; then every other day thereafter. Maintenance: Highly individualized. To treat ulcerative colitis ENEMA(HYDROCORTISONE)
Adults. 100 mg every night for 2 to 3 wk or until condition improves. Route Onset Peak Duration P.O. Unknown 1 hr 1.25– 1.5 days P.O.|| Unknown 1–2 hr Unknown I.V.§ Rapid Unknown Unknown I.M. Unknown 4–8 hr Unknown I.M. Rapid 1 hr Unknown I.M.§ Rapid 1 hr Variable Other* Unknown 24–48 hr 3 days– 4 wk

Mechanism of Action

Binds to intracellular glucocorticoid receptors and suppresses inflammatory and immune responses by:

inhibiting neutrophil and monocyte accumulation at inflammation site and suppressing their phagocytic and bactericidal activity

stabilizing lysosomal membranes hydrocortisone 507 G H I Hydrocortisone Phosphate §Succinate ||Cypionate * Acetate; intra-articular, intralesional, and soft-tissue injection.

suppressing antigen response of macrophages and helper T cells

inhibiting synthesis of cellular mediators of inflammatory response, such as cytokines, interleukins, and prostaglandins.

Contraindications

Hypersensitivity to hydrocortisone or its components, idiopathic thrombocytopenic purpura (I.M.), intestinal conditions prohibiting intrarectal steroids (P.R.), recent live-virus vaccination, systemic fungal infection

Interactions

acetaminophen: Increased risk of hepatotoxicity amphotericin B, carbonic anhydrase inhibitors: Possibly severe hypokalemia anabolic steroids, androgens: Increased risk of edema and severe acne anticholinergics: Possibly increased intraocular pressure anticoagulants, thrombolytics: Increased risk of GI ulceration and hemorrhage, possibly decreased therapeutic effects of these asparaginase: Increased risk of hyperglycemia and toxicity aspirin,
NSAIDs: Increased risk of GI distress and bleeding cholestyramine: Possibly increased hydrocortisone clearance cyclosporine: Possibly increased action of both ; increased risk of seizures digoxin: Possibly hypokalemia-induced arrhythmias and digitalis toxicity ephedrine, phenobarbital, phenytoin, rifampin: Decreased blood hydrocortisone level estrogens, oral contraceptives: Increased therapeutic and toxic effects of hydrocortisone insulin, oral antidiabetic : Possibly increased blood glucose level isoniazid: Possibly decreased therapeutic effects of isoniazid macrolide antibiotics: Possibly decreased hydrocortisone clearance
mexiletine: Decreased blood mexiletine level neuromuscular blockers: Possibly increased neuromuscular blockade, causing respiratory depression or apnea potassium-depleting , such as thiazide diuretics: Possibly severe hypokalemia potassium supplements: Possibly decreased effects of these supplements somatrem, somatropin: Possibly decreased therapeutic effects of these streptozocin: Increased risk of hyperglycemia vaccines: Decreased antibody response and increased risk of neurologic complications
alcohol use: Increased risk of GI distress and bleeding

Side Efect

CNS: Ataxia, behavioral changes, depression, dizziness, euphoria, fatigue, headache, increased intracranial pressure with papilledema, insomnia, malaise, mood changes, paresthesia, seizures, steroid psychosis, syncope, vertigo
CV: Arrhythmias (from hypokalemia), fat embolism, heart failure, hypertension, hypotension, thromboembolism, thrombophlebitis
EENT: Exophthalmos, glaucoma, increased intraocular pressure, nystagmus, posterior subcapsular cataracts
ENDO: Adrenal insufficiency during stress, cushingoid symptoms (buffalo hump, central obesity, moon face, supraclavicular fat pad enlargement), diabetes mellitus, growth suppression in children, hyperglycemia, negative nitrogen balance from protein catabolism
GI: Abdominal distention; hiccups; increased appetite; nausea; pancreatitis; peptic ulcer; rectal abnormalities, such as bleeding, blistering, burning, itching, or pain (rectal form); ulcerative esophagitis; vomiting
GU: Amenorrhea, glycosuria, menstrual irregularities, perineal burning or tingling
HEME: Easy bruising, leukocytosis
MS: Arthralgia; aseptic necrosis of femoral and humeral heads; compression fractures; muscle atrophy, twitching, or weakness; myalgia; osteoporosis; spontaneous fractures; steroid myopathy; tendon rupture
SKIN: Acne; altered skin pigmentation; diaphoresis; erythema; hirsutism; necrotizing vasculitis; petechiae; purpura; rash; scarring; sterile abscess; striae; subcutaneous fat atrophy; thin, fragile skin; urticaria
Other: Anaphylaxis, hypocalcemia, hypokalemia, hypokalemic alkalosis, impaired wound healing, masking of signs of infection, metabolic alkalosis, suppressed skin test reaction, weight gain hydrocortisone 508

Cautions

Systemic hydrocortisone shouldn’t be given to immunocompromised patients, such as those with fungal and other infections, including amebiasis, hepatitis B, tuberculosis, vaccinia, and varicella.

Give daily dose of hydrocortisone in morning to mimic normal peak in adrenocortical secretion of corticosteroids.

When possible, give oral dose with food or milk to avoid GI distress.

Don’t give acetate injectable suspension by I.V. route.

Give hydrocortisone sodium succinate as a direct I.V. injection over 30 seconds to several minutes, or as an intermittent or a continuous infusion. For infusion, dilute to 1 mg/ml or less with D5W, normal saline solution, or dextrose 5% in normal saline solution.

Inject I.M. form deep into gluteal muscle, and rotate injection sites to prevent muscle atrophy. Subcutaneous injection may cause atrophy and sterile abscess.

Shake foam container vigorously for 5 to 10 seconds before each use. Gently withdraw applicator plunger past the fill-line on the applicator barrel while container is upright on a level surface. Administer rectal foam only with provided applicator. After each use, wash applicator, container cap, and underlying tip with warm water.

High-dose therapy shouldn’t be given for longer than 48 hours. Be alert for depression and psychotic episodes.

Monitor weight, blood pressure, and electrolyte levels regularly during therapy.

Expect hydrocortisone to worsen infections or mask signs and symptoms.

Monitor blood glucose level in diabetic patients, and increase insulin or oral antidiabetic drug dosage, as prescribed.

Know that elderly patients are at high risk for osteoporosis during long-term therapy.

Anticipate the possibility of acute adrenal insufficiency with stress, such as emotional upset, fever, surgery, or trauma. Increase hydrocortisone dosage, as prescribed.
WARNING Avoid withdrawing drug suddenly after long-term therapy because adrenal crisis can result. Expect to reduce dosage gradually and monitor response.

PATIENT SAFTY

Advise patient to take daily dose of hydrocortisone at 9 a.m.

Instruct patient to take tablets or oral suspension with milk or food.

Teach patient how to use foam or enema form, if prescribed.

Caution patient not to stop drug abruptly without first consulting prescriber.

Instruct patient to report early evidence of adrenal insufficiency: anorexia, difficulty breathing, dizziness, fainting, fatigue, joint pain, muscle weakness, and nausea.

Inform patient that he may bruise easily.

Advise patient on long-term therapy to have periodic eye examinations.

If patient receives long-term therapy, urge her to carry or wear medical identification.

Caution patient to avoid people with infections because drug can suppress immune system, increasing risk of infection. If patient comes into contact with chickenpox or measles, instruct him to call prescriber because he may need prophylactic care.

Category

Chemical class: Phenanthrene derivative, semisynthetic opioid derivative
Therapeutic class: Analgesic

Pregnancy category: C

Controlled substance schedule: II

Indications

To relieve moderate to severe pain

ORALL

Adults.2.5 to 10 mg every 3 to 6 hr, p.r.n.
Adults.2 mg every 3 to 6 hr, p.r.n. Increased to 4 mg or more every 4 to 6 hr, if indicated.
Adults. Highly individualized and dependent on patient’s previous total daily 24-hour opioid use. Once dosage is determined, hydromorphone hydrochloride 509 G H I drug is given daily.
I.V.INJECTION
Adults.1 mg every 3 hr, p.r.n. I.M.OR SUBCUTANEOUS INJECTION
Adults.1 or 2 mg every 3 to 6 hr, p.r.n. Increased to 3 or 4 mg every 4 to 6 hr, if needed for severe pain. SUPPOSITORIES
Adults.3 mg every 4 to 8 hr, p.r.n. Route Onset Peak Duration P.O. 30 min 1.5–2 hr 4 hr I.V. 10–15 15–30 min 2–3 hr min I.M. 15 min 30–60 min 4–5 hr SubQ 15 min 30–90 min 4 hr P.R. 30 min Unknown 4 hr

Mechanism of Action

May bind with opioid receptors in the spinal cord and higher levels in the CNS. In this way, hydromorphone is believed to stimulate mu and kappa receptors, thus altering the perception of and emotional response to pain.

Contraindications

Acute asthma; hypersensitivity to hydromorphone, other narcotics, or their components; increased intracranial pressure; severe respiratory depression; upper respiratory tract obstruction

Interactions

anticholinergics: Increased risk of ileus, severe constipation, or urine retention antihypertensives, diuretics, guanadrel, guanethidine, mecamylamine: Increased risk of orthostatic hypotension barbiturate anesthetics: Increased sedative effect of hydromorphone belladonna alkaloids, difenoxin and atropine, diphenoxylate and atropine, kaolin pectin, loperamide, paregoric: Increased risk of CNS depression and severe constipation buprenorphine, butorphanol, dezocine, nalbuphine, pentazocine: Possibly potentiated or suppressed symptoms of spontaneous opioid withdrawal CNS depressants, other opioid analgesics: Additive CNS depression and hypotension hydroxyzine: Increased analgesia, CNS depression, and hypotension metoclopramide: Decreased effect of metoclopramide on GI motility naloxone: Possibly withdrawal symptoms in physically dependent patients
naltrexone: Possibly prolonged respiratory depression or cardiac arrest neuromuscular blockers: Additive CNS depression
alcohol use: Increased CNS depression

Side Efect

CNS: Anxiety, confusion, dizziness, drowsiness, euphoria, hallucinations, headache, nervousness, restlessness, sedation, somnolence, tremor, weakness
CV: Hypertension, orthostatic hypotension, palpitations, tachycardia
EENT: Blurred vision, diplopia, dry mouth, laryngeal edema, laryngospasm, nystagmus, tinnitus
GI: Abdominal cramps, anorexia, biliary tract spasm, constipation, hepatotoxicity, nausea, vomiting
GU: Dysuria, urine retention
RESP: Dyspnea, respiratory depression, wheezing
SKIN: Diaphoresis, flushing
Other: Injection site pain, redness, and swelling; physical and psychological dependence

Cautions

To improve analgesic action, give hydromorphone before pain becomes intense.

Give I.V. form by direct injection over at least 2 minutes. For infusion, mix drug with D5W, normal saline solution, or Ringer’s solution.

Monitor patient for respiratory depression when using I.V. route. Keep resuscitation equipment and naloxone nearby.

Rotate I.M. and subcutaneous injection sites.

Monitor effectiveness of hydromorphone in relieving pain; consult prescriber as needed.

Assess patient for constipation.

Monitor patient for evidence of physical dependence or abuse.

Anticipate that drug may mask or worsen gallbladder pain.

Be aware that all other around-the-clock opioid analgesics should be stopped when capsules are prescribed. Expect to give hydromorphone hydrochloride 510 immediate-release nonopioid analgesics for exacerbation of pain and for preventing pain during certain activities.

PATIENT SAFTY

Instruct patient to take drug exactly as prescribed and before pain is severe.

Advise patient to take drug with food to avoid GI distress.

Tell patient not to break open or chew capsules but to swallow them whole.

Instruct patient to refrigerate suppositories.

Caution patient to avoid alcohol and OTC during therapy, unless prescriber approves.

Instruct patient to report constipation, difficulty breathing, severe nausea, or vomiting.

Inform patient that drug may cause drowsiness and sedation. Advise her to avoid hazardous activities until drug’s CNS effects are known.

Tell patient to change position slowly to minimize orthostatic hypotension.

To avoid withdrawal, instruct physically dependent patient not to stop taking hydromorphone abruptly.

Category

Chemical class: 4-aminoquinoline compound
Therapeutic class: Antiprotozoal, antirheumatic, lupus erythematosus suppressant

Pregnancy category: C

Indications

To prevent malaria
Adults. 400 mg the same day of each week starting 2 wk before entering endemic area and continuing until departure from endemic area. If this isn’t possible, initially 800 mg in two divided doses 6 hr apart, followed 1 wk later with 400 mg and then 400 mg on same day of each week thereafter until departure from endemic area. Infants and children. 5 mg/kg the same day of each week, starting 2 wk before entering endemic area and continuing until departure from endemic area. If this isn’t possible, initially 10 mg/kg in two divided doses 6 hr apart, followed 1 wk later with 5 mg/kg and then 5 mg/kg on same day of each week thereafter until departure from endemic area. Maximum: Adult dosage. To treat acute attacks of malaria caused by Plasmodium vivax, P. malariae, P. ovale, and susceptible strains of P. falciparum
Adults. Initial: 800 mg, followed by 400 mg in 6 to 8 hr and 400 mg on next 2 consecutive days. Or, 800 mg given as a single dose or an initial dose of 10 mg base/kg (maximum, 620 mg base [800 mg]), followed by 5 mg base/kg (maximum, 310 mg base [400 mg]) 6 hr after first dose, 5 mg base/kg 18 hr after second dose, and 5 mg base/kg 24 hr after third dose. Infants and children. Initial: 10 mg base/kg (maximum, 620 mg base [800 mg]), followed by 5 mg base/kg (maximum, 310 mg base [400 mg]) 6 hr after first dose, 5 mg base/kg 18 hr after second dose, and 5 mg base/kg 24 hr after third dose. To treat chronic discoid and systemic lupus erythematosus
Adults. Initial: 400 mg once or twice daily for several weeks or months. Maintenance: 200 to 400 mg daily. To treat acute or chronic rheumatoid arthritis
Adults. Initial: 400 to 600 mg daily for 4 to 12 wk. Maintenance: 200 mg to 400 mg daily.
DOSAGE ADJUSTMENT For patients with rheumatoid arthritis who develop troublesome

Side Efect

, initial dosage decreased for 5 to 10 days and then gradually increased to optimum response level.

Mechanism of Action

May mildly suppress the immune system, inhibiting production of rheumatoid factor and acute phase reactants. Hydroxychloroquine also accumulates in WBCs, stabilizing lysosomal membranes and inhibiting enzymes such as collagenase and proteases that cause cartilage breakdown. These actions may decrease symptoms of rheumahydroxychloroquine sulfate 511 G H I toid arthritis and lupus erythematosus. Hydroxychloroquine also binds to and alters DNA of malaria parasite to prevent it from reproducing. It also may increase the pH of acid vesicles, which interferes with vesicle function and may inhibit parasitic phospholipid metabolism in erythrocytes, thereby halting plasmodial activity.

Contraindications

Hypersensitivity to 4-aminoquinoline compounds (including hydroxychloroquine), long-term therapy in children, retinal or visual changes related to 4-aminoquinoline compounds

Interactions

aurothioglucose: Increased risk of blood dyscrasias digoxin: Increased digoxin concentrations

Side Efect

CNS: Abnormal nerve conduction, ataxia, dizziness, emotional lability, headache, irritability, lassitude, nervousness, neuromuscular sensory abnormalities, nightmares, psychosis, seizures, vertigo
CV: Cardiomyopathy (prolonged high doses)
EENT: Abnormal pigmentation (bullseye appearance) or colored vision, blurred vision, central scotoma with decreased visual acuity, corneal deposits, decreased corneal sensitivity, diplopia, irreversible retinal damage (in lupus erythematosus or rheumatoid arthritis), halo vision, lassitude, macular edema or atrophy, nerve-related hearing loss, nystagmus, pericentral or paracentral scotoma, photophobia, retinal fundus changes, tinnitus, visual abnormalities
ENDO: Hypoglycemia
GI: Abdominal cramps, anorexia, diarrhea, elevated liver function test results, fulminant hepatic failure, nausea, vomiting
HEME: Agranulocytosis, aplastic anemia, hemolysis (in patients with glucose-6-phosphate dehydrogenase [G6PD] deficiency), leukopenia, thrombocytopenia
MS: Atrophy of proximal skeletal muscle groups, depressed tendon reflexes, muscle weakness
RESP: Bronchospasm
SKIN: Acute generalized exanthematous pustulosis, alopecia, altered mucosal and skin pigmentation, bleaching of hair, dermatitis (including exfoliative dermatitis), non–light-sensitive psoriasis, pruritus, psoriasis exacerbation, rash, Stevens-Johnson syndrome, urticaria
Other: Angioedema, porphyria, weight loss

Cautions

Use hydroxychloroquine cautiously in patients with G6PD deficiency, patients with hepatic disease or alcoholism, and patients taking hepatotoxic .

Monitor children closely for adverse reactions because they’re especially sensitive to 4-aminoquinoline compounds.

Observe patients with psoriasis closely because hydroxychloroquine may lead to severe psoriasis attack. Also monitor patients with porphyria closely because hydroxychloroquine may worsen it. Expect to use hydroxychloroquine in patients with psoriasis or porphyria only after risks and benefits have been considered.

During prolonged therapy, obtain periodic blood cell counts, as ordered, to detect adverse hematologic effects. Expect to stop drug if severe adverse effects occur.

Monitor patient’s vision when giving hydroxychloroquine for lupus erythematosus or rheumatoid arthritis because irreversible retinal damage may occur in some patients during long-term or high-dose therapy. Ask regularly about vision abnormalities, such as light flashes or streaks, that may indicate retinopathy. Expect patient to have an initial ophthalmologic examination, followed by examinations every 3 months. Report changes to prescriber immediately, and expect drug to be stopped. Retinal changes may progress even after therapy stops.

Monitor patient on long-term therapy for muscle weakness and abnormal knee and ankle reflexes. If present, notify prescriber and expect drug to be stopped.

Expect drug to be stopped if patient with rheumatoid arthritis shows no improvement, such as reduced joint swelling or increased mobility, in 6 months.

If serious

Side Efect

occur, notify prescriber immediately. Expect drug to be stopped. Also expect to give ammonium chloride (8 g daily in divided doses for adults) 3 or 4 days weekly for several months because acidification of urine hydroxychloroquine sulfate 512 increases renal excretion of drug.

PATIENT SAFTY

Instruct patient to take drug with meals or milk to minimize stomach upset.

Tell patient to take hydroxychloroquine exactly as prescribed because taking too much may cause serious

Side Efect

and taking too little or skipping doses decreases effectiveness.

Caution patient to notify prescriber about troublesome

Side Efect

. Hydroxychloroquine dosage may need to be adjusted or drug stopped.

Caution patient who takes drug for rheumatoid arthritis or lupus erythematosus about possible visual reactions and the need for periodic eye examinations. Tell patient to notify prescriber about abnormal visual changes, including blurred vision, halos around lights, and light flashes or streaks; explain that drug will need to be stopped.

Tell patient receiving prolonged therapy about the need for periodic blood tests to detect adverse effects.

Advise patient to notify prescriber if muscle weakness develops.

Category

Chemical class: Piperazine derivative
Therapeutic class: Antianxiety, antiemetic, antihistamine, sedative-hypnotic

Pregnancy category: C

Indications

To relieve anxiety and induce sedation and hypnosis , ORAL SUSPENSION, SYRUP, Adults and adolescents.50 to 100 mg as a single dose. Children.600 mcg/kg as a single dose.
I.M.INJECTION Adults and adolescents.50 to 100 mg every 4 to 6 hr, p.r.n. (antianxiety); 50 mg as a single dose (sedative-hypnotic). To treat pruritus , ORAL SUSPENSION, SYRUP, Adults and adolescents. 25 to 100 mg t.i.d. or q.i.d., p.r.n. Children.500 mcg/kg every 6 hr, p.r.n. To provide antiemetic effects , ORAL SUSPENSION, SYRUP, Adults and adolescents. 25 to 100 mg t.i.d. or q.i.d., p.r.n. Children.500 mcg/kg every 6 hr, p.r.n.
I.M.INJECTION Adults and adolescents.25 to 100 mg, p.r.n. Children.1.1 mg/kg as a single dose. As adjunct to permit reduction in preoperative and postoperative opioid dosage
I.M.INJECTION Adults and adolescents.25 to 100 mg given with prescribed opioid. Children. 1.1 mg/kg given with prescribed opioid.
DOSAGE ADJUSTMENT For elderly patients, treatment is started at lowest possible dosage. Route Onset Peak Duration P.O. 15–60 min Unknown 4–6 hr I.M. 20–30 min Unknown 4–6 hr

Mechanism of Action

Competes with histamine for histamine1 receptor sites on surfaces of effector cells. This suppresses results of histaminic activity, including edema, flare, and pruritus. Hydroxyzine’s antiemetic effect may stem from central anticholinergic actions. Sedative actions occur at subcortical level of CNS and are dose-related.

Contraindications

Breast-feeding; early pregnancy; hypersensitivity to cetirizine, hydroxyzine, or their components

Interactions

CNS depressants: Increased CNS depression
alcohol use: Increased CNS depression

Side Efect

CNS: Drowsiness, hallucinations, headache, hydroxyzine 513 G H I involuntary motor activity, seizures, tremor
EENT: Dry mouth
SKIN: Pruritus, rash, urticaria
Other: Allergic reaction, injection site pain

Cautions

Don’t give hydroxyzine by subcutaneous or I.V. route because tissue necrosis may occur.

Inject I.M. form deep into large muscle, using Z-track method.

Observe for oversedation if patient takes another CNS depressant.

PATIENT SAFTY

Urge patient to avoid alcohol.

Caution patient about drowsiness; tell her to avoid hazardous activities until drug’s CNS effects are known.

Instruct woman to tell prescriber if she is or could be pregnant because drug is contraindicated in early pregnancy.

Category

Chemical class: Belladonna alkaloid, tertiary amine
Therapeutic class: Antimuscarinic, antispasmodic

Pregnancy category: C

Indications

To treat peptic ulcers and GI tract disorders caused by spasm ELIXIR, Adults and adolescents. 0.125 to 0.25 mg every 4 to 6 hr. Children.Dosage individualized by weight. Adults and adolescents. 0.375 mg every 12 hr. Adults and adolescents. 0.375 to 0.75 mg every 12 hr. Maximum: 1.5 mg daily. Adults and adolescents. 0.125 to 0.5 mg t.i.d. or q.i.d. Children. Dosage individualized by weight. I.V., I.M., OR SUBCUTANEOUS INJECTION Adults and adolescents. 0.25 to 0.5 mg every 4 to 6 hr. Children.Dosage individualized by weight. To control salivation and excessive secretions during surgical procedures
I.V.INJECTION Adults and adolescents.0.5 mg 30 to 60 min before procedure. Route Onset Peak Duration P.O.* 20–30 30–60 4 hr min min P.O.() 20–30 40–90 12 hr min min I.V., I.M., 2–3 15–30 4 hr SubQ min min

Mechanism of Action

Competitively inhibits acetylcholine at autonomic postganglionic cholinergic receptors. Because the most sensitive receptors are in salivary, bronchial, and sweat glands, hyoscyamine acts mainly to reduce salivary, bronchial, and sweat gland secretions. It also causes GI smooth muscle to contract and decreases gastric secretion and GI motility. It also causes bladder detrusor muscle to contract, reduces nasal and oropharyngeal secretions, and decreases airway resistance from relaxation of smooth muscle in the bronchi and bronchioles.

Contraindications

Acute hemorrhage and hemodynamic instability; angle-closure glaucoma; hepatic disease; hypersensitivity to hyoscyamine, other anticholinergics, or their components; ileus; intestinal atony; myasthenia gravis; myocardial ischemia; obstructive GI disease; obstructive uropathy; renal disease; severe ulcerative colitis; tachycardia; toxic megacolon

Interactions

anticholinergics: Possibly increased antihyoscyamine sulfate 514 * For tablets only; for elixir and oral solution, onset is 5 to 20 min, and peak and duration are unknown. For tablets only; for capsules, onset and peak are unknown, and duration is 12 hr. cholinergic effects antidiarrheals (adsorbent): Possibly decreased hyoscyamine effects calciumand magnesium-containing antacids, carbonic anhydrase inhibitors, citrates, sodium bicarbonate, urinary alkalinizers: Possibly potentiated therapeutic and adverse effects of hyoscyamine
haloperidol: Possibly decreased haloperidol effects
ketoconazole: Possibly reduced ketoconazole absorption metoclopramide: Possibly antagonized therapeutic effects of metoclopramide opioid analgesics: Increased risk of severe constipation and ileus

Side Efect

CNS: Drowsiness, insomnia
EENT: Blurred vision; dry mouth, nose, and throat; photophobia
ENDO: Decreased lactation
GI: Constipation
GU: Impotence, urine retention
SKIN: Decreased sweating
Other: Heatstroke, injection site redness and urticaria

Cautions

Use hyoscyamine cautiously in patients who have arrhythmias, autonomic neuropathy, coronary artery disease, heart failure, hiatal hernia with reflux esophagitis, hypertension, hyperthyroidism, renal failure, or tachycardia.

Give drug 30 to 60 minutes before meals and at bedtime. Give bedtime dose at least 2 hours after last meal of day.

Anticipate that tablets may not disintegrate and may appear in stool.
WARNING Anticipate an increased risk of drug-induced heatstroke in hot or humid weather because hyoscyamine decreases sweating.
WARNING Be aware that lower doses may paradoxically decrease heart rate. Higher doses affect nicotinic receptors in autonomic ganglia, causing delirium, disorientation, hallucinations, and restlessness.

Monitor urine output, and be alert for urine retention.

PATIENT SAFTY

Instruct patient to void before taking each dose and to notify prescriber if she has trouble urinating during therapy.

Advise patient to take drug 30 to 60 minutes before meals and at bedtime. Bedtime dose should be taken at least 2 hours after last meal of the day.

Explain that drug may cause drowsiness. Advise patient to avoid hazardous activities until drug’s CNS effects are known.

If patient reports dry mouth, suggest using sugarless hard candy or gum.

Inform male patient that drug may cause impotence. If it occurs, suggest that he discuss it with prescriber.

Advise patient to avoid exposure to high temperatures and to increase fluid intake, unless contraindicated.

Category

Chemical class: Propionic acid derivative
Therapeutic class: Analgesic, antiinflammatory, antipyretic

Pregnancy category: C

(before 30 weeks gestation); D (starting at 30 weeks gestation)

Indications

To relieve pain in rheumatoid arthritis and osteoarthritis ,CHEWABLE ,ORAL SUSPENSION,
Adults.300 mg q.i.d., or 400, 600, or 800 mg t.i.d. or q.i.d. Range: 1.2 to 3.2 g daily. To relieve mild to moderate pain ,CHEWABLE ,ORAL SUSPENSION,
Adults. 400 mg every 4 to 6 hr, p.r.n.
IV:
Adults. 400 to 800 mg infused over at least 30 minutes, every 6 hours, as needed. To relieve acute migraine pain ibuprofen 515 G H I ,CHEWABLE ,ORAL SUSPENSION,
Adults. 200 to 400 mg at onset of migraine pain. Maximum: 400 mg daily. To relieve pain in primary dysmenorrhea ,CHEWABLE ,ORAL SUSPENSION,
Adults. 400 mg every 4 hr, p.r.n. To relieve pain in juvenile arthritis ,CHEWABLE ,ORAL SUSPENSION, Children. 30 to 70 mg/kg daily in divided doses t.i.d. or q.i.d.; 20 mg/kg daily for mild disease. To relieve minor aches, pains, and dysmenorrhea and to reduce fever ,CHEWABLE ,ORAL SUSPENSION,
Adults. 200 to 400 mg every 4 to 6 hr. Maximum: 1.2 g daily. To relieve moderate to severe pain as an adjunct to opioid analgesics
IV:
Adults.400 mg to 800 mg infused over at least 30 minutes, every 6 hours, as needed. To reduce fever ,CHEWABLE ,ORAL SUSPENSION, Children ages 6 months to 12 years. 5 to 10 mg/kg every 4 to 6 hr. Maximum: 40 mg/ kg daily.
IV:
Adults.400 mg infused over at least 30 minutes, followed by 400 mg infused over at least 30 minutes, every 4 to 6 hours. Or, 100 to 200 mg infused over at least 30 minutes, every 4 hours, as needed. Route Onset Peak Duration P.O.* 30 min Unknown 4–6 hr P.O. Up to 7 days 1–2 wk Unknown P.O. In 1 hr 2–4 hr 6–8 hr

Mechanism of Action

Blocks activity of cyclooxygenase, the enzyme needed to synthesize prostaglandins, which mediate inflammatory response and cause local vasodilation, swelling, and pain. By inhibiting prostaglandins, this NSAID reduces inflammatory symptoms and relieves pain. Ibuprofen’s antipyretic action probably stems from its effect on the hypothalamus, which increases peripheral blood flow, causing vasodilation and encouraging heat dissipation.

Contraindications

Angioedema, asthma, bronchospasm, nasal polyps, rhinitis, or urticaria caused by hypersensitivity to aspirin, ibuprofen, iodides, or other NSAIDs; perioperative pain with coronary artery bypass graft surgery

Interactions

acetaminophen: Possibly increased renal effects with long-term use of both antihypertensives: Decreased effectiveness of these aspirin: Possibly decreased cardioprotective and stroke-preventive effects of aspirin aspirin, other
NSAIDs: Increased risk of bleeding and adverse GI effects bone marrow depressants: Possibly increased leukopenic and thrombocytopenic effects of bone marrow depressants cefamandole, cefoperazone, cefotetan: Increased risk of hypoprothrombinemia and bleeding colchicine, platelet aggregation inhibitors: Increased risk of GI bleeding, hemorrhage, and ulcers corticosteroids, potassium supplements: Increased risk of adverse GI effects cyclosporine: Increased risk of nephrotoxicity from both , increased blood cyclosporine level digoxin: Increased blood digoxin level and risk of digitalis toxicity diuretics (loop, potassium-sparing, and thiazide): Decreased diuretic and antihypertensive effects gold compounds, nephrotoxic : Increased risk of adverse renal effects heparin, oral anticoagulants, thrombolytics: Increased anticoagulant effects, increased risk of hemorrhage insulin, oral antidiabetics: Possibly increased hypoglycemic effects of these lithium: Increased blood lithium level methotrexate: Decreased methotrexate clearance and increased risk of toxicity plicamycin,
valproic acid: Increased risk of ibuprofen 516 * For analgesic effects. For anti-inflammatory effects. For antipyretic effects. hypoprothrombinemia and GI bleeding, hemorrhage, and ulcers probenecid: Possibly increased blood level, effectiveness, and risk of toxicity of ibuprofen
alcohol use: Increased risk of adverse GI effects

Side Efect

CNS: Aseptic meningitis, dizziness, headache, nervousness, seizures, stroke
CV: Fluid retention, heart failure, hypertension, MI, peripheral edema, tachycardia
EENT: Amblyopia, epistaxis, stomatitis, tinnitus
GI: Abdominal cramps, distention, or pain; anorexia; constipation; diarrhea; diverticulitis; dyspepsia; dysphagia; elevated liver function test results; epigastric discomfort; esophagitis; flatulence; gastritis; gastroenteritis; gastroesophageal reflux disease; GI bleeding, hemorrhage, perforation, or ulceration; heartburn; hemorrhoids; hepatic failure; hepatitis; hiatal hernia; indigestion; melena; nausea; stomatitis; vomiting
GU: Cystitis, hematuria, renal failure (acute)
HEME: Agranulocytosis, anemia, aplastic anemia, eosinophilia, hemolytic anemia, leukopenia, neutropenia, pancytopenia, prolonged bleeding time, thrombocytopenia
RESP: Bronchospasm, dyspnea, wheezing
SKIN: Blisters, erythema multiforme, photosensitivity, pruritus, rash, StevensJohnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, flulike symptoms, hypokalemia, weight gain

Cautions

Use ibuprofen with extreme caution in patients with a history of ulcer disease or GI bleeding because NSAIDs such as ibuprofen increase risk of GI bleeding and ulceration. Expect to use ibuprofen for shortest time possible in these patients.

Risk of serious cardiovascular thrombotic events such as a MI or stroke increases the longer ibuprofen is used. Expect to give drug for shortest time possible.

For I.V. use, dilute Caldolor brand of ibuprofen to final concentration of 4 mg/ ml or less using 0.9% sodium chloride injection, 5% dextrose injection, or lactated Ringer’s solution. For an 800-mg dose, dilute 8 ml Caldolor in at least 200 ml diluent; for a 400-mg dose, dilute 4 ml Caldolor in at least 100 ml diluent. Diluted solutions may be kept at room temperature up to 24 hours. When infusing ibuprofen intravenously, infusion time must be at least 30 minutes.

Serious GI tract ulceration, bleeding, and perforation may occur without
WARNING symptoms. Elderly patients are at greater risk. To minimize risk, give oral drug with food. If GI distress occurs, withhold drug and notify prescriber immediately.

Use ibuprofen cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.
WARNING Monitor patient closely for thrombotic events, including MI and stroke, because NSAIDs increase the risk.

Monitor patient—especially if he’s elderly or receiving long-term oral ibuprofen therapy—for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results because, in rare cases, elevations may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in elderly patients, patients taking diuretics or ACE inhibitors, and patients with heart failure, impaired renal function, or hepatic dysfunction; drug may cause renal failure.

Monitor CBC for decreased hemoglobin and hematocrit. Drug may worsen anemia.
WARNING If patient has bone marrow suppression or is receiving an antineoplastic drug, monitor laboratory results (including WBC count), and watch for evidence of infection. Ibuprofen’s anti-inflammatory and antipyretic actions may mask signs and symptoms, such as fever and pain.

Assess patient’s skin regularly for signs of rash or other hypersensitivity reaction because ibuprofen is an NSAID and may cause serious skin reactions without warning, even in patients with no history of NSAID sensivitity. At first sign of reaction, ibuprofen 517 G H I stop drug and notify prescriber.

Although analgesic effect occurs at low doses, expect to give at least 400 mg four times daily for anti-inflammatory effect.

Expect higher doses for rheumatoid arthritis than for osteoarthritis.

Be aware that ibuprofen oral suspension may contain sucrose, which may affect blood glucose level in diabetic patients.

PATIENT SAFTY

Instruct patient to take tablets with a full glass of water, and caution him not to lie down for 15 to 30 minutes to prevent esophageal irritation.

Advise patient to take drug with food or after meals to reduce GI distress.

Urge patient no more drug or for longer time than prescribed because stomach bleeding may occur and risk of MI or stroke may increase.

Instruct patient to consult prescriber if he needs to take drug for more than 3 days for fever or 10 days for pain; if stomach problems (heartburn, upset, pain) recur; if he has a history of ulcers, bleeding problems, hypertension, or heart or renal disease; if he takes a diuretic; or if he’s over age 65.

Inform patient with phenylketonuria that Motrin chewable tablets contain aspartame.

Inform patient that full therapeutic effect for arthritis may take 2 weeks or longer.

Urge patient to avoid taking two different NSAIDs at the same time, unless directed, and to alert prescriber before taking ibuprofen if he has ever had an allergic reaction to any other analgesic or feverreducing drug or has a history of asthma.

Urge patient to avoid alcohol, aspirin, and corticosteroids while taking ibuprofen, unless prescribed. If patient takes aspirin as prevention of MI or stroke, explain that ibuprofen may interfere with this effect.

Suggest that patient wear sunscreen and protective clothing when outdoors.

Advise patient to report flulike symptoms, rash, signs of GI bleeding, swelling, vision changes, and weight gain.

Urge parents to tell prescriber promptly if child receiving drug develops a severe or persistent sore throat, high fever, headache, persistent diarrhea, nausea, or vomiting or hasn’t been drinking fluids.

Advise parents to consult prescriber before giving OTC ibuprofen to a child if the child has asthma, ulcers, bleeding problems, high blood pressure, heart or kidney disease, a need for diuretic therapy, serious adverse effects from previous use of fever reducers or pain relievers, or persistent stomach problems, such as heartburn, upset stomach, or stomach pain.

Caution pregnant patient not to take NSAIDs such as ibuprofen during last trimester because they may cause premature closure of the ductus arteriosus.

Explain that ibuprofen may increase risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.

Explain that ibuprofen may increase risk of serious adverse GI reactions; stress importance of seeking immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.

Alert patient to rare but serious skin reactions. Urge him to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity.

Category

Chemical: Methanesulfonanilide derivative Therapeutic: Class III antiarrhythmic

Pregnancy category: C

Indications

To rapidly convert recent-onset atrial flutter or fibrillation to sinus rhythm
IV: Adults weighing 60 kg (132 lb) or more. 1 mg over 10 min. Dose repeated 10 min after first dose is finished if arrhythmia persists. Adults weighing less than 60 kg. 0.01 mg/ kg over 10 min. Dose is repeated 10 min after first dose is completed if arrhythmia persists.
DOSAGE ADJUSTMENT Infusion stopped if arrhythmia is terminated or if sustained or ibutilide fumarate 518 nonsustained ventricular tachycardia or prolonged QT or QTc interval develops.

Mechanism of Action

May promote sodium movement through slow inward sodium channels in myocardial cell membranes. Ibutilide also may inhibit potassium channels in myocardial cell membranes involved in cardiac repolarization. These actions prolong cardiac action potential by delaying repolarization and increasing atrial and ventricular refractoriness. As a result, sinus rate slows and AV conduction is delayed.

Contraindications

Hypersensitivity to ibutilide or components

Interactions

amiodarone, astemizole, disopyramide, maprotiline, phenothiazines, procainamide, quinidine, sotalol, tricyclic antidepressants: Possibly prolonged QT interval, leading to increased risk of proarrhythmias

Side Efect

CNS: Headache, syncope
CV: AV block, bradycardia, bundle-branch block, heart failure, hypertension, hypotension, idioventricular rhythm, orthostatic hypotension, palpitations, prolonged QT interval, sinus and supraventricular tachycardia, supraventricular arrhythmias, ventricular arrhythmias, ventricular tachycardia (sustained and nonsustained)
GI: Nausea
GU: Renal failure

Cautions

Before giving ibutilide, check serum electrolyte levels and expect to correct abnormalities, as prescribed. Be especially alert for hypokalemia and hypomagnesemia, which can lead to arrhythmias.

Give drug undiluted or dilute in 50 ml normal saline solution or D5W. Add contents of 10-ml vial (0.1 mg/ml) to 50 ml solution to obtain 0.017 mg/ml. Use polyvinyl chloride plastic bags or polyolefin bags for admixtures. Give drug within 24 hours (48 hours if refrigerated).

Infuse drug slowly over 10 minutes.

As ordered, monitor patient’s cardiac rhythm continuously during infusion and for at least 4 hours afterward—longer if arrhythmias appear or if patient has abnormal hepatic function. Observe patient for ventricular ectopy.

Make sure defibrillator and to treat sustained ventricular tachycardia are available during therapy and when monitoring patient after therapy.

PATIENT SAFTY

Inform patient that ibutilide will be given by I.V. infusion and that his heart rhythm will be monitored continuously.

Ask patient to report chest pain, faintness, numbness, tingling, palpitations, and shortness of breath.

Advise patient to keep follow-up appointments to monitor heart rhythm.

Category

Chemical class: Piperidinyl-benzisoxazole derivative
Therapeutic class: Second-generation antipsychotic; atypical antipsychotic

Pregnancy category: C

Indications

To treat schizophrenia
Adults. Initial: 1 mg twice daily, adjusted to target dosage range as follows: 2 mg twice daily on day 2, 4 mg twice daily on day 3, and 6 mg twice daily on day 4. Dosage may be further increased, if needed, as follows: 8 mg twice daily on day 5, 10 mg twice daily on day 6, and 12 mg twice daily on day 7. Maximum: 12 mg b.i.d. twice daily.
DOSAGE ADJUSTMENT For patients taking strong CYP2D6 or CYP3A4 inhibitors, dosage reduced by half. Route Onset Peak Duration P.O. 1–2 wk 2–4 hr Unknown

Mechanism of Action

Selectively blocks serotonin type 2 (5-HT2) and dopamine type 2 (D2) receptors in CNS, thereby suppressing psychotic symptoms.

Contraindications

Hypersensitivity to iloperidone or its components iloperidone 519 G H I

Interactions

antibiotics such as fluoroquinolones or macrolides, class I A antiarrhythmics such as procainamide or quinidine, class III antiarrhythmics such as amiodarone or sotalol, other antipsychotic such as chlorpromiazine or thioridazine, or any other drug that affects the QT interval such as methadone or pentamidine: Possibly prolonged QT interval antihyertensive : Increased antihypertensive effects CYP3A4 inhibitors such as ketoconazole, CYP2D6 inhibitors such as fluoxetine or paroxetine: Increased plasma iloperidone level dextromethorphan: Increased blood dextromethorphan level

Side Efect

CNS: Aggression, delusion, dizziness, extrapyramidal effects, fatigue, lethargy, seizures, somnolence, suicidal ideation, restlessness, tremor
CV: CHF, orthostatic hypotension, palpitations, QT-interval prolongation, tachycardia
EENT: Blurred vision, conjunctivitis, dry mouth, nasal congestion, nasopharyngitis, upper respiratory tract infection
ENDO: Diabetic ketoacidosis, elevated prolactin levels, hyperglycemia, hyperosmolar coma
GI: Abdominal discomfort, diarrhea, nausea
GU: Ejaculation failure, erectile dysfunction, priapism, urinary incontinence
HEME: Leukopenia
MS: Arthralgia, musculoskeletal stiffness, spasms, myalgia
RESP: Dyspnea
SKIN: Rash
Other: Weight gain

Cautions

Iloperidone shouldn’t be used in patients with a history of cardiovascular disease such as QT-interval prolongation, recent MI, uncompensated heart failure, or cardiac arrhythmias. It also shouldn’t be used in patients taking other known to prolong the QT interval and in patients with hepatic impairment.
WARNING Iloperidone shouldn’t be used to treat patients with dementia-related psychosis, especially elderly patients, because of an increased risk of death.

Use cautiously in patients who have a history of seizures or who have conditions that lower the seizure threshold, such as Alzheimer’s dementia. Also use cautiously in patients at risk for aspiration pneumonia.

Expect to start
DOSAGE ADJUSTMENT schedule in patients who have been off iloperidone therapy for more than 3 days.

Obtain baseline serum potassium and magnesium levels in patients at risk for electrolyte imbalances, and then monitor periodically throughout therapy, as ordered, because electrolyte imbalances increase risk of prolonged QT interval or arrhythmia. If patient reports dizziness, palpitations, or syncope, notify prescriber and expect further evaluation to be done.
WARNING Neuroleptic malignant syndrome has occurred in patients taking other antipsychotic . Monitor patient for hyperpyrexia, muscle rigidity, altered mental status, and autonomic instability. If present, notify prescriber immediately, expect drug to be discontinued, and start intensive treatment, as prescribed. Watch for recurrence if patient resumes antipsychotic therapy.

Monitor patient for tardive dyskinesia, which has occurred with other antipsychotic . If patient develops involuntary, dyskinetic movements, notify prescriber and expect to discontinue drug.

Monitor blood glucose level, especially in patients with diabetes mellitus, because iloperidone may alter blood glucose enough to induce life-threatening ketoacidosis or hyperosmolar coma.

Monitor patient’s CBC periodically, as ordered, especially during first few months of therapy, because iloperidone may cause neutropenia. Also, be aware that other antipyschotic have caused sometimes fatal leukopenia and agranulocytosis. If patient’s WBC count decreases, expect drug to be discontinued.

Monitor patient closely for abnormal tendencies that may suggest suicidal thinking, especially when iloperidone therapy starts or dosage is changed.

PATIENT SAFTY

Inform patient that when iloperidone therapy starts, dosage must be adjusted for up to a week to reach target level. Also iloperidone 520 explain that adjustment process will need to be repeated if she skips drug for more than 3 days.

Advise patient or caregiver o notify prescriber about unusual, severe, or persistent

Side Efect

because drug may need to be discontinued.

Urge patient or caregiver to report evidence of abnormal thinking, especially when therapy starts or dosage changes.

Tell diabetic patient to monitor blood glucose levels closely and to report persistent elevations immediately to prescriber.

Caution patient to avoid hazardous activities until CNS effects of drug are known. Patient should also avoid alcohol.

Instruct patient to avoid activities that might raise body temperature, such as doing strenuous exercise, being exposed to extreme heat, taking other with anticholinergic activity, or being subjected to dehydration.

Stress the need to comply with follow-up appointments and laboratory tests.

Tell patient to rise slowly from lying to sitting position and from sitting position to standing to avoid dizziness or lightheadedness during therapy.

Category

Chemical class: Synthetic analogue of prostacyclin PGI2
Therapeutic class: Pulmonary arterial antihypertensive

Pregnancy category: C

Indications

To improve symptoms and exercise tolerance and prevent further deterioration from pulmonary arterial hypertension in patients with Class III or IV symptoms INHALATION SOLUTION
Adults. Initial: 2.5 mcg as one-time dose. If tolerated well for 2 hr, dosage increased to 5 mcg. Maintenance: 5 mcg six to nine times daily during waking hours with at least 2 hr between each dose. Maximum: 45 mcg daily.

Mechanism of Action

Dilates systemic and pulmonary arterial vascular beds, which lowers blood pressure in pulmonary arterial system.

Contraindications

Hypersensitivity to iloprost or its components

Interactions

anticoagulants: Increased risk of bleeding antihypertensives, vasodilators: Increased hypotensive effect

Side Efect

CNS: Apathy, dizziness, headache, insomnia, restlessness, syncope
CV: Chest pain, congestive heart failure, hypotension, palpitations, peripheral edema, supraventricular tachycardia, thrombosis, vasodilation
EENT: Epistaxis, gingival bleeding, tongue pain
ENDO: Hyperglycemia
GI: Abdominal cramps, diarrhea, nausea, vomiting
GU: Renal failure
MS: Back pain, muscle cramps or spasms
RESP: Bronchospasm, dyspnea, hemoptysis, increased cough, pneumonia, wheezing
SKIN: Flushing
Other: Flulike symptoms, increased alkaline phosphatase level

Cautions

Use iloprost cautiously in patients with hepatic or renal impairment.

Give iloprost only with the Prodose AAD System, a pulmonary drug delivery device. Avoid letting solution contact skin or eyes.
WARNING Don’t give drug if patient’s systolic blood pressure is less than 85 mm Hg.

Notify prescriber if patient develops exertional syncope because dosage may need to be adjusted.
WARNING Stop iloprost immediately if patient develops evidence of pulmonary edema, such as shortness of breath, anxiety, restlessness, and abnormal breath sounds. Notify prescriber, and provide supportive care, as prescribed.

Monitor patient’s vital signs while starting therapy because drug may cause syncope.

Assess patient’s compliance with treatment regimen. If patient has repeatedly lengthiloprost 521 G H I ened treatment times, resulting in incomplete dosing, notify prescriber. A different strength may be ordered that decreases inhalation time, which may help increase compliance.

PATIENT SAFTY

Instruct patient to use iloprost inhalation therapy exactly as prescribed. Tell patient that at least 2 hours must elapse between doses but that benefits of iloprost may not last 2 hours, so he should adjust times of administration to cover planned activities.

Teach patient how to administer iloprost using Prodose AAD System. Tell patient to have a backup system available in case of equipment malfunction.

Advise patient to stand up slowly because drug may cause dizziness or faintness. If these symptoms persist or worsen, tell patient to notify prescriber because a DOSAGE ADJUSTMENT may be required.

Category

Chemical class: Dibenzazepine derivative
Therapeutic class: Antidepressant

Pregnancy category: Not rated

Indications

To treat depression
Adults. Initial: 75 mg daily at bedtime, gradually increased as needed and tolerated. Maximum: 300 mg daily (hospitalized patients), 200 mg/day (outpatients).
Adults. Initial: 25 to 50 mg t.i.d. or q.i.d., gradually increased as needed and tolerated. Maximum: 300 mg daily (hospitalized patients), 200 mg daily (outpatients).
DOSAGE ADJUSTMENT Initial dosage reduced to 25 mg at bedtime for depressed elderly patients; then adjusted as needed and tolerated up to 100 mg daily in divided doses. Adolescents. Initial: 25 to 50 mg daily in divided doses, adjusted as needed and tolerated. Maximum: 100 mg daily. Children ages 6 to 12. 10 to 30 mg daily in divided doses b.i.d. As adjunct to treat childhood enuresis Children age 6 and over. 25 mg 1 hr before bedtime. Increased to 50 mg if no response occurs within 1 wk and child is under age 12; increased to 75 mg if child is age 12 or over. Maximum: 2.5 mg/kg daily. Route Onset Peak Duration P.O. 2–3 wk* Unknown Unknown

Mechanism of Action

May interfere with reuptake of serotonin (and possibly other neurotransmitters) at presynaptic neurons, thus enhancing serotonin’s effects at postsynaptic receptors. Mood elevation may result from restoration of normal levels of neurotransmitters at nerve synapses. This tricyclic antidepressant also blocks acetylcholine receptors, which may explain how it relieves enuresis.

Contraindications

Acute recovery period after MI; hypersensitivity to imipramine, other tricyclic antidepressants, or their components; use within 2 weeks of MAO inhibitor therapy

Interactions

amantadine, anticholinergics, antidyskinetics, antihistamines: Risk of increased anticholinergic effects, including confusion, hallucinations, and nightmares anticonvulsants: Increased risk of CNS depression, increased risk of seizures, decreased effectiveness of imipramine antithyroid : Possibly agranulocytosis barbiturates, carbamazepine: Possibly decreased imipramine level and effects cimetidine, fluoxetine: Possibly increased blood imipramine level clonidine, guanadrel, guanethidine: Possibly decreased antihypertensive effects of these , increased CNS depression (clonidine) imipramine 522 * For antidepressant effect.
CNS depressants: Increased CNS depression, respiratory depression, and hypotension disulfiram, ethchlorvynol: Risk of delirium, increased CNS depression (ethchlorvynol) estramustine, estrogen-containing oral contraceptives, estrogens: Risk of increased bioavailability of imipramine, increased depression
MAO inhibitors: Increased risk of hypertensive crisis, severe seizures, and death oral anticoagulants: Possibly increased anticoagulant activity pimozide, probucol: Risk of arrhythmias sympathomimetics (including ophthalmic epinephrine and vasoconstrictive local anesthetics): Increased risk of arrhythmias, hyperpyrexia, hypertension, tachycardia thyroid hormones: Risk of increased therapeutic and adverse effects of both
alcohol use: Increased CNS depression, increased alcohol effects sun exposure: Increased risk of photosensitivity

Side Efect

CNS: Anxiety, ataxia, chills, confusion, delirium, dizziness, drowsiness, excitation, extrapyramidal reactions, fever, hallucinations, headache, insomnia, nervousness, nightmares, parkinsonism, seizures, stroke, suicidal ideation, tremor
CV: Arrhythmias, orthostatic hypotension, palpitations
EENT: Blurred vision, dry mouth, increased intraocular pressure, pharyngitis, taste perversion, tinnitus, tongue swelling
ENDO: Gynecomastia, syndrome of inappropriate ADH secretion
GI: Constipation, diarrhea, heartburn, ileus, increased appetite, nausea, vomiting
GU: Impotence, libido changes, testicular swelling, urine retention
HEME: Agranulocytosis, bone marrow depression
RESP: Wheezing
SKIN: Alopecia, diaphoresis, jaundice, photosensitivity, pruritus, rash, urticaria
Other: Allergic reaction, facial edema, weight gain

Cautions

Use imipramine cautiously in patients with a history of urine retention or angleclosure glaucoma because drug’s anticholinergic effects may cause urine retention and increased intraocular pressure.
WARNING Don’t give MAO inhibitors within 2 weeks of imipramine. Patient may experience hypertensive crisis, seizures, and death.

Frequently assess for

Side Efect

during first 2 hours of therapy.

Check supine and standing blood pressure for orthostatic hypotension before and during imipramine therapy and before dosage increases.

Anticipate increased risk of arrhythmias in patients with a history of cardiac disease.

When drug is used for depression, expect mood elevation to take 2 to 3 weeks. Watch patient closely for suicidal tendencies, especially children and adolescents and especially when therapy starts or dosage changes, because depression may worsen temporarily at these times.

Avoid abrupt withdrawal of drug in patients on long-term therapy. Such withdrawal may cause headache, malaise, nausea, sleep disturbance, and vomiting.

Taper drug gradually, as ordered, a few days before surgery to avoid risk of hypertension during surgery.

Obtain CBC, as ordered, if patient experiences signs and symptoms of infection, such as fever or pharyngitis.

Limit amount of drug given to potentially suicidal patient.

PATIENT SAFTY

Advise patient to take imipramine exactly as prescribed. Warn that stopping drug abruptly may cause headache, malaise, nausea, trouble sleeping, and vomiting.

Caution parents to monitor child or adolescent closely for suicidal tendencies, especially when therapy starts or dosage changes.

Urge patient to report chills, trouble urinating, dizziness, excess sedation, fever, palpitations, signs of allergic reaction, and sore throat.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Urge patient to avoid alcohol during imipramine therapy because it increases CNS depression and alcohol effects.

Suggest that patient eat small, frequent meals to help relieve nausea.

Instruct patient to avoid prolonged expoimipramine 523 G H I sure to sunlight because of the risk of photosensitivity.

Inform male patient about possible impotence and increased or decreased libido.

If patient reports dry mouth, suggest sugarless candy or gum to relieve it. Tell him to check with prescriber if dry mouth persists after 2 weeks.

Category

Chemical class: Polyvalent antibody
Therapeutic class: Antibacterial, anti–Kawasaki disease agent, antipolyneuropathy agent, antiviral, immunizing agent, platelet count stimulator

Pregnancy category: C

Indications

To treat primary immunodeficiency
I.M.INJECTION(BAYGAM)
Adults. 0.66 ml/kg (at least 200 mg/kg) every 3 to 4 wk; initial dose may be doubled.
IV:(GAMIMUNE N5% S/D OR10% S/D)
Adults.100 to 200 mg/kg every mo. If response is inadequate, dose may be increased to as much as 400 mg/kg or dosing frequency may be increased.
IV:(GAMMAGARD S/D, POLYGAM S/D)
Adults. 200 to 400 mg/kg initially, then at least 100 mg/kg every mo thereafter. If response is inadequate, dose or frequency may be adjusted.
IV:(GAMMAR-P IV)
Adults. 200 to 400 mg/kg every 3 to 4 wk. Adolescents and children. 200 mg/kg every 3 to 4 wk.
IV:(GAMUNEX10%)
Adults. 300 to 600 mg/kg every 3 or 4 wk.
IV:(IVEEGAM EN)
Adults. 200 mg/kg every mo.
IV:(OCTAGAM5%)
Adults. Initial: 30 mg/kg/hr for first 30 minutes; increased, if tolerated, to 60 mg/kg/hr for second 30 minutes and, if tolerated, to 120 mg/kg/hr for another 30 minutes; followed by maintenance infusion of up to 200 mg/kg/hr.
IV:(SANDOGLOBULIN) Adults and children. 200 mg/kg every mo. If response is inadequate, dose may be increased to 300 mg/kg or dosing frequency may be increased.
IV:(VENOGLOBULIN-I) Adults and children. 200 mg/kg every mo. If response is inadequate, dose may be increased to 300 to 400 mg/kg every mo or dosing frequency may be increased.
IV:(VENOGLOBULIN-S5% OR10%) Adults and children.200 mg/kg every mo. If response is inadequate, dose may be increased to as much as 400 mg/kg or dosing frequency may be increased. To treat primary immunodeficiency disorders associated with defects in humoral immunity
IV:(GAMMAGARD LIQUID) Adults and children.300 to 600 mg/kg daily every 3 to 4 wk. To treat idiopathic thrombocytopenic purpura (ITP)
IV:(GAMIMUNE N5% S/D) Adults and children. 400 mg/kg daily for 5 days. Or, 1,000 mg/kg for 1 or 2 days for patients not at risk for increased fluid volume.
IV:(GAMIMUNE N10% S/D) Adults and children. 1,000 mg/kg for 1 or 2 days for patients not at risk for increased fluid volume.
IV:(GAMUNEX10%)
Adults. 1 g/kg daily for 2 consecutive days (second dose may be withheld if adequate immune globulin 524 increase in platelet count occurs 24 hours after first dose). Or, 0.4 g/kg daily for 5 consecutive days.
DOSAGE ADJUSTMENT In acute ITP of childhood, I.V. Sandoglobulin therapy may be discontinued after second day of 5-day course if initial platelet count response is adequate (30,000 to 50,000/mm3). In chronic ITP, an additional I.V. infusion of 400 mg/kg (of either Sandoglobulin or Gamimune) may be prescribed if platelet count falls below 30,000/mm3or if patient develops significant bleeding. If response remains inadequate, an additional I.V. infusion of 800 to 1,000 mg/kg may be given.
IV:(GAMMAGARD S/D)
Adults.1 g/kg. If response is inadequate, up to three separate doses may be administered on alternate days.

IV

(RHOPHYLAC)
Adults. 50 mcg/kg at 2 ml/15 to 60 seconds.
IV:(SANDOGLOBULIN) Adults and adolescents. 400 mg/kg daily for 2 to 5 consecutive days.
IV:(VENOGLOBULIN-I) Adults and children.Induction: Cumulative dose up to 2 g/kg over 2 to 7 consecutive days. Maintenance (adults): 2 g/kg as a single dose every 2 wk as needed to maintain platelet count above 30,000/mm3or prevent bleeding episodes. Maintenance (children): 1 g/kg as a single dose every 2 wk as needed to maintain platelet count above 30,000/mm3or prevent bleeding episodes.
IV:(VENOGLOBULIN-S5% OR10%) Adults and children. Cumulative dose up to 2,000 mg/kg over 5 consecutive days.
DOSAGE ADJUSTMENT An additional I.V. infusion of 1,000 mg/kg may be administered to maintain a platelet count of 30,000/mm3in children or 20,000/mm3in adults or to prevent bleeding episodes. To treat acute or chronic pediatric ITP; to treat chronic adult-onset ITP; to treat prediatricand adult-onset ITP secondary to HIV infection
I.V.INJECTION(WINRHO SDF) Adults and children.Initial: 250 international units/kg given as a single injection over 3 to 5 min. Or, 125 international units/kg given as a single injection over 3 to 5 min and repeated once on a separate day. Maintenance: Frequency and dosage highly individualized based on patient’s hemoglobin and platelet levels.
DOSAGE ADJUSTMENT For patients with hemoglobin level less than 10 g/dl, dose reduced to 125 to 200 international units/kg. As adjunct to treat Kawasaki disease
IV:(GAMMAGARD S/D) Adults and adolescents. 1 g/kg as a single dose; or, 400 mg/kg daily for 4 consecutive days.
IV:(IVEEGAM EN,VENOGLOBULIN-S5% OR10%) Adults and adolescents.2 g/kg as a single dose; or, Iveegam EN may be given at 400 mg/kg daily for 4 days. To decrease the risk of graft-versus-host disease, interstitial pneumonia, septicemia, and other infections during first 100 days after bone marrow transplantation
IV:(GAMIMUNE N5% S/D OR10% S/D) Adults over age 20. 500 mg/kg on 7th and 2nd days before transplant (or at time when conditioning therapy for transplantation begins), and then weekly through 90th day after transplant. As adjunct to treat bacterial infections secondary to B-cell chronic lymphocytic leukemia
IV:(GAMMAGARD S/D, POLYGAM S/D) Adults and adolescents. 400 mg/kg every 3 to 4 wk. To prevent bacterial infection in children with HIV who are immunosuppressed
IV:(GAMIMUNE N5% S/D OR10% S/D) Children. 400 mg/kg daily every 28 days. To prevent hepatitis A
I.M.INJECTION(BAYGAM) Adults with household or institutional contacts. 0.02 ml/kg (0.01 ml/lb). Adults traveling to areas where hepatitis A is common. 0.02 ml/kg if staying less than 3 mo, 0.06 ml/kg (repeated every 4 to 6 mo) if staying 3 mo or longer. To prevent or lessen severity of measles (rubeola) in susceptible persons
I.M.INJECTION(BAYGAM)
Adults. 0.2 ml/kg (0.11 ml/lb) for persons exposed fewer than 6 days previously. To provide passive immunization against varicella in immunosuppressed patients
I.M.INJECTION(BAYGAM)
Adults. 0.6 to 1.2 ml/kg if varicella-zoster immune globulin (human) is unavailable. immune globulin 525 G H I To reduce the risk of infection and fetal damage in women who have been exposed to rubella in early pregnancy
I.M.INJECTION(BAYGAM)
Adults. 0.55 ml/kg. To suppress Rh isoimmunization
I.M.INJECTION,
IV:(RHOPHYLAC) Adult pregnant women. 1,500 international units as a single dose at 28 to 30 wk gestation followed by 1,500 international units within 72 hr after delivery of an Rh-positive newborn.
I.M.INJECTION(WINRHO SDF) Adult pregnant women. 1,500 international units as a single dose at 28 wk gestation followed by 600 international units within 72 hr after delivery of an Rh-positive newborn.
I.V.INJECTION(WINRHO SDF) Adult pregnant women. 1,500 international units as a single dose infused over 3 to 5 min at 28 wk gestation followed by 600 international units over 3 to 5 min within 72 hr after delivery of an Rh-positive newborn.
DOSAGE ADJUSTMENT For patients more than 34 wk gestation and having an abortion, amniocentesis, or other manipulative procedure, 600 international units given within 72 hr but preferably immediately after procedure. For patients 34 wk gestation or less and having amniocentesis or chorionic villus sampling, 1,500 international units given immediately after procedure and repeated every 12 wk for duration of pregnancy. For patients with threatened abortion at any stage of pregnancy, 1,500 international units given immediately. To treat incompatible blood transfusions
I.M.INJECTION,
IV:(RHOPHYLAC) Adults exposed to Rh-positive RBCs. 100 international units/2 ml transfused blood or 1 ml erythrocyte concentrate within 72 hr of exposure.
I.M.INJECTION(WINRHO SDF) Adults exposed to Rh-positive whole blood. 6,000 international units every 12 hr until total dose (60 international units/ml of blood) is given. Adults exposed to Rh-positive RBCs. 6,000 international units every 12 hr until total dose (120 international units/ml of cells) is given.
I.V.INJECTION(WINRHO SDF) Adults exposed to Rh-positive whole blood. 3,000 international units infused over 3 to 5 min every 8 hr until total dose (45 international units/ml of blood) is given. Adults exposed to Rh-positive RBCs. 3,000 international units infused over 3 to 5 min every 8 hr until total dose (90 international units/ml of cells) is given. To treat massive fetomaternal hemorrhage
I.M.INJECTION,
IV:(RHOPHYLAC) Adults exposed to Rh-positive RBCs. 1,500 international units plus 100 international units for every 1 ml of fetal RBCs exceeding 15 ml if transplacental bleeding is quantified or an additional 1,500 international units if transplacental bleeding can’t be quantified within 72 hours of hemorrhage.
I.M.INJECTION(WINRHO SDF) Adults exposed to Rh-positive whole blood. 6,000 international units every 12 hr until total dose (60 international units/ml of blood) is given. Adults exposed to Rh-positive RBCs. 6,000 international units every 12 hr until total dose (120 international units/ml of cells) is given.
I.V.INJECTION(WINRHO SDF) Adults exposed to Rh-positive whole blood. 3,000 international units infused over 3 to 5 min every 8 hr until total dose (45 international units/ml of blood) is given. Adults exposed to Rh-positive RBCs. 3,000 international units infused over 3 to 5 min every 8 hr until total dose (90 international units/ml of cells) is given. Route Onset Peak Duration I.V. Unknown Unknown 21–28 days

Mechanism of Action

Releases antibody-specific globulins to produce an antibody-antigen reaction that results in bacterial lysis and facilitates bacterial phagocytosis. In treatment of ITP, immune globulin blocks iron receptors on macrophages to increase immunoglobulin action. Immune globulin also increases cytokine production and improves B-cell immune function by regulating T-cell and macrophage activity. Newly formed antigenimmune globulin 526 antibody complexes produce split complement components that cause bacterial lysis. In Kawasaki disease and bacterial infections with B-cell chronic lymphocytic leukemia, immune globulin neutralizes bacterial and viral toxins that harm immune and inflammatory responses.

Incompatibilities

Don’t mix immune globulin with any other , including other immune globulins, or with any I.V. solutions other than D5W or manufacturer’s supplied diluent because effects of doing so are unknown.

Contraindications

Hypersensitivity to immune globulin (human) or its components, IgA deficiency in patients with known antibody to IgA

Interactions

live-virus vaccines: Possibly decreased response to vaccine

Side Efect

CNS: Headache, malaise
CV: Tachycardia
GI: Nausea, vomiting
MS: Arthralgia, back pain, myalgia
RESP: Dyspnea

Cautions

Before giving immune globulin, monitor patient’s fluid volume and BUN and serum creatinine levels, as ordered, to determine risk for acute renal failure. Those at increased risk include patients with renal insufficiency, diabetes mellitus, volume depletion, sepsis, or paraproteinemia; those taking nephrotoxic ; and those over age 65. Expect drug to be discontinued if renal function deteriorates.

When preparing immune globulin, verify that appropriate form is being used— either immune globulin intramuscular for I.M. injection or immune globulin intravenous for I.V. infusion.

To reconstitute drug (except Gammagard Liquid, which doesn’t need reconstitution), follow manufacturer’s guidelines and use only diluent recommended by manufacturer. Don’t shake solution; excessive shaking causes foaming. If drug or diluent is cold, drug may take up to 20 minutes to dissolve.

If drug is reconstituted outside of sterile laminar airflow conditions, administer it immediately and discard unused portions.

Consult manufacturer’s guidelines to determine appropriate flow rate for starting infusion. Expect to increase flow rate after 15 to 30 minutes, as specified.

When giving drug by I.M. injection, inject it only into deltoid muscle of upper arm or anterolateral aspect of upper thigh. If giving a dose larger than 5 ml, divide it and administer at separate sites.
WARNING Watch for an acute inflammatory reaction in patients who have never received immune globulin therapy before, in those whose last treatment was more than 8 weeks before, and in those whose initial infusion rate exceeded 1 ml/minute. Within 30 minutes to 1 hour after beginning of infusion, assess for chills, fever, facial flushing, feeling of tightness in chest, dizziness, nausea, vomiting, diaphoresis, and hypotension. Notify prescriber immediately if such symptoms occur, and be prepared to stop infusion until symptoms have subsided.
WARNING After immune globulin administration, monitor patient closely for aseptic meningitis. Notify prescriber if patient develops drowsiness, fever, nausea, vomiting, nuchal rigidity, photophobia, painful eye movements, or severe headache.

Be aware that immune globulin intravenous is made from human plasma and therefore may contain infectious agents, such as viruses. Risk of transmitting a virus by infusion has been reduced by screening blood donors, testing donated blood, and inactivating or removing certain viruses from the product.

For patient receiving WinRho SDF to treat ITP, assess clinical response by monitoring patient’s platelet count, RBC count, hemoglobin level, and reticulocyte level.

For patient receiving WinRho SDF for exposure to incompatible blood transfusions or massive fetal hemorrhage, give drug within 72 hours of incident.

PATIENT SAFTY

Instruct patient to immediately report any symptoms he experiences after receiving immune globulin.

Inform patient to postpone live-virus vaccinations for up to 11 months after receivimmune globulin 527 G H I ing immune globulin because drug may delay or inhibit response to vaccine.

Category

Chemical class: Bipyridine derivative
Therapeutic class: Cardiac inotrope

Pregnancy category: C

Indications

To treat heart failure in patients who haven’t responded sufficiently to digoxin, diuretics, or vasodilators
IV:
Adults.Initial: 0.75 mg/kg by bolus over 2 to 3 min and repeated after 30 min, if needed. Maintenance: 5 to 10 mcg/ kg/min by infusion. Maximum: 10 mg/kg daily. Route Onset Peak Duration I.V. 2–5 min In 10 min 30 min–2 hr

Mechanism of Action

Inhibits phosphodiesterase enzymes that normally degrade myocardial cAMP. This action increases intracellular levels of cAMP, which regulates intracellular and extracellular calcium balance. Increased intracellular cAMP level enhances influx of calcium into cell, thereby increasing force of myocardial contractions. Inamrinone also acts directly on peripheral vascular smoothmuscle cells, causing relaxation and dilation, which reduces preload and afterload.

Incompatibilities

Don’t administer inamrinone through same I.V. line as furosemide because precipitate may form. Don’t dilute inamrinone in solution that contains dextrose because a chemical interaction occurs over 24 hours.

Contraindications

Hypersensitivity to inamrinone, bisulfites, or their components; severe aortic or pulmonary valvular disease

Interactions

disopyramide: Possibly severe hypotension

Side Efect

CNS: Fever
CV: Chest pain, hypotension, pericarditis, supraventricular tachycardia, ventricular arrhythmias
GI: Abdominal pain, anorexia, elevated liver function test results, hepatotoxicity, nausea, vomiting
HEME: Elevated erythrocyte sedimentation rate, thrombocytopenia (especially with high-dose or prolonged treatment)
MS: Myositis
RESP: Hypoxemia, pleuritis
SKIN: Jaundice
Other: Infusion site burning

Cautions

WARNING Be aware that inamrinone may increase risk of ventricular arrhythmias in patients with atrial flutter or fibrillation. To minimize risk, expect to pretreat such patients with digoxin.

Give drug undiluted or diluted in normal or half-normal (0.45) saline solution to a concentration of 1 to 3 mg/ml, as prescribed. Use diluted solution within 24 hours.
WARNING Monitor vital signs regularly. If blood pressure falls significantly, slow or stop infusion and notify prescriber.

Monitor weight, cardiac index, central venous pressure, pulmonary artery wedge pressure, and fluid intake and output as appropriate to assess drug’s effectiveness.
WARNING Assess often for signs of thrombocytopenia, such as bruising or bleeding and altered platelet count. If signs appear, expect to decrease inamrinone dose or discontinue drug.

PATIENT SAFTY

Instruct patient to notify you or another nurse if he becomes dizzy, which may indicate hypotension.

Category

Chemical class: Sulfonamide inamrinone;indapamide 528
Therapeutic class: Antihypertensive, diuretic

Pregnancy category: B

Indications

To treat edema caused by heart failure
Adults.2.5 mg daily in the morning, increased to 5 mg daily after 1 wk, if indicated. To manage hypertension
Adults.2.5 mg daily, increased to 5 mg after 4 wk, if needed. Route Onset Peak Duration P.O.* 1–2 hr Unknown 36 hr P.O. 1–2 wk 8–12 wk Up to 8 wk

Mechanism of Action

Acts mainly on distal convoluted tubules, where it enhances excretion of sodium, chloride, and water by inhibiting sodium ion movement across renal tubules. The resulting decrease in plasma and extracellular fluid volume decreases peripheral vascular resistance and reduces blood pressure. This thiazide diuretic also may cause arterial vasodilation by blocking calcium channels in smooth-muscle cells.

Contraindications

Anuria; hypersensitivity to thiazide or related diuretics or to sulfonamide-derived

Interactions

amiodarone: Increased risk of arrhythmias if hypokalemia develops cholestyramine, colestipol: Decreased indapamide absorption diazoxide: Increased risk of hyperglycemia digoxin: Increased risk of digitalis toxicity if hypokalemia develops hypotension-producing : Increased antihypertensive or diuretic effects lithium: Increased risk of lithium toxicity neuromuscular blockers: Possibly increased neuromuscular blockade, risk of respiratory depression oral anticoagulants: Possibly decreased anticoagulant effects

Side Efect

CNS: Anxiety, dizziness, drowsiness, fatigue, fever, headache, mood changes, nervousness, sleep disturbance, vertigo, weakness
CV: Arrhythmias, hypercholesterolemia, orthostatic hypotension, palpitations
EENT: Dry mouth
ENDO: Hyperglycemia, hypoglycemia
GI: Anorexia, constipation, diarrhea, hepatitis, nausea, pancreatitis, thirst, vomiting
GU: Impotence, nocturia
MS: Gout, muscle spasms
SKIN: Jaundice, necrotizing vasculitis, photosensitivity, pruritus, rash, urticaria
Other: Dilutional hypochloremia and hyponatremia, hypokalemia, metabolic alkalosis, weight loss

Cautions

Administer indapamide with food or milk to reduce adverse GI reactions.

Give drug early in the day to avoid nocturia.

Weigh patient daily, and monitor fluid intake and output, blood pressure, and serum electrolyte levels, especially in elderly women, because severe hyponatremia and hypokalemia may occur. Hypokalemia also commonly occurs in patients taking diuretics. Report electrolyte abnormalities, and expect to provide corrective measures, as prescribed.

Monitor BUN and serum creatinine levels regularly, as appropriate.

If muscle cramps and weakness develop from hypokalemia, expect prescriber to order potassium supplement or potassiumsparing diuretic.

When managing hypertension, expect therapeutic response to indapamide to take several weeks.

PATIENT SAFTY

Advise patient to take indapamide early in the day to avoid nighttime urination and to take it with food or milk to minimize GI distress.

Encourage patient to eat high-potassium , such as oranges and bananas.

Caution patient to change position slowly to minimize effects of orthostatic hypotension.

Instruct patient to weigh himself daily at the same time and wearing similar clothing. Direct him to report a weight gain of more than 2 lb (0.9 kg) per day or 5 lb indapamide 529 G H I * For edema. For hypertension (with multiple doses). (2.3 kg) per week.

Inform patient about possible photosensitivity.

If patient has a dry mouth, suggest sugarless gum or hard candy to relieve it.

Category

Chemical class: Indoleacetic acid derivative
Therapeutic class: Antigout, antiinflammatory, antirheumatic

Pregnancy category: Not rated

Indications

To relieve symptoms of ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis , ORAL SUSPENSION
Adults.25 to 50 mg b.i.d. to q.i.d., increased by 25 or 50 mg daily every wk, if needed. Maximum: 200 mg daily. After adequate response, dosage reduced as low as possible. (ANTIRHEUMATIC)
Adults.75 mg daily, increased to 75 mg b.i.d, if needed. SUPPOSITORIES
Adults.50 mg up to q.i.d. To relieve symptoms of acute gouty arthritis , ORAL SUSPENSION
Adults.Initial: 100 mg. Increased up to 50 mg t.i.d. Maximum: 200 mg daily. After pain is relieved, dosage tapered until drug is discontinued. SUPPOSITORIES
Adults. 50 mg up to q.i.d. Maximum: 200 mg daily. To treat inflammation and relieve acute shoulder pain from bursitis or tendinitis , ORAL SUSPENSION
Adults. 75 to 150 mg daily in divided doses t.i.d. or q.i.d. for 7 to 14 days. SUPPOSITORIES
Adults.50 mg up to q.i.d. Maximum: 200 mg daily.
DOSAGE ADJUSTMENT Dosage reduced for elderly patients. To treat hemodynamically significant patent ductus arteriosus in premature infants weighing 500 to 1,750 g (1 to 3.9 lb)
I.V.INJECTION Infants over age 7 days. Initial: 200 mcg/kg (0.2 mg/kg) over 5 to 10 sec; 1 or 2 additional doses of 250 mcg/kg (0.25 mg/kg) given at 12to 24-hr intervals, if needed. Neonates ages 2 to 7 days. Initial: 200 mcg/ kg (0.2 mg/kg) over 5 to 10 sec; 1 or 2 additional doses of 200 mcg/kg (0.2 mg/kg) given at 12to 24-hr intervals, if needed. Neonates under age 48 hours. Initial: 200 mcg/kg (0.2 mg/kg) over 5 to 10 sec; 1 or 2 additional doses of 100 mcg/kg (0.1 mg/kg) given at 12to 24-hr intervals, if needed. Route Onset Peak Duration P.O.* 2–4 hr 2–5 days Unknown P.O. 30 min Unknown 4–6 hr P.O. In 7 days 1–2 wk Unknown

Mechanism of Action

Blocks activity of cyclooxygenase, the enzyme needed to synthesize prostaglandins, which mediate inflammatory response and cause local vasodilation, swelling, and pain. By blocking cyclooxygenase and inhibiting prostaglandins, this NSAID reduces inflammatory symptoms and helps relieve pain.

Incompatibilities

Don’t give indomethacin suspension with alkaline antacids or liquids. Don’t mix reconstituted indomethacin sodium with I.V. infusion solutions.

Contraindications

Allergy or hypersensitivity to aspirin, indomethacin, iodides, other NSAIDs, or their components; history of proctitis or recent rectal bleeding (suppositories) indomethacin 530 * For antigout effects. For anti-inflammatory effects. For antirheumatic effects.

Interactions

Note: All effects listed are for oral forms and suppositories unless indicated. acetaminophen: Increased risk of adverse renal effects (long-term use of both ) aluminumand magnesium-containing antacids: Possibly decreased blood indomethacin level aminoglycosides: Increased risk of aminoglycoside toxicity antihypertensives: Decreased effectiveness of these aspirin, other
NSAIDs: Increased risk of adverse GI effects and non-GI bleeding bone marrow depressants: Possibly increased leukopenic or thrombocytopenic effects of these cefamandole, cefoperazone, cefotetan: Increased risk of hypoprothrombinemia and bleeding colchicine, platelet aggregation inhibitors: Increased risk of GI bleeding, hemorrhage, and ulcers corticosteroids, potassium supplements: Increased risk of adverse GI effects cyclosporine: Increased risk of nephrotoxicity from both , increased blood cyclosporine level diflunisal: Increased blood indomethacin level and risk of GI bleeding digoxin: Increased blood digoxin level and risk of digitalis toxicity (all forms) diuretics (thiazide, loop, and potassiumsparing): Decreased diuretic and antihypertensive effects gold compounds, nephrotoxic : Increased risk of adverse renal effects heparin, oral anticoagulants, thrombolytics: Possibly increased anticoagulant effects and risk of hemorrhage lithium: Increased blood lithium level and risk of toxicity methotrexate: Increased risk of methotrexate toxicity plicamycin,
valproic acid: Increased risk of hypoprothrombinemia and GI bleeding, hemorrhage, and ulcers probenecid: Increased blood level and effectiveness of indomethacin, increased risk of indomethacin toxicity zidovudine: Increased blood zidovudine level and risk of toxicity, increased risk of indomethacin toxicity
alcohol use: Increased risk of adverse GI effects

Side Efect

Note: All reactions are for oral forms and suppositories unless indicated.
CNS: Confusion, depression, dizziness, drowsiness, fatigue, hallucinations, headache, intraventricular hemorrhage (I.V.), peripheral neuropathy, seizures, stroke, syncope, vertigo
CV: Arrhythmias, chest pain, edema, fluid retention (all forms), heart failure, hypertension, MI, pulmonary hypertension (I.V.), tachycardia
EENT: Blurred vision, corneal and retinal damage, epistaxis, hearing loss, tinnitus
ENDO: Hypoglycemia (I.V.)
GI: Abdominal cramps or pain, abdominal distention (I.V.), anorexia, constipation, diarrhea, diverticulitis, dyspepsia, dysphagia, epigastric discomfort, esophagitis, gastric perforation, gastritis, gastroenteritis, gastroesophageal reflux disease, GI bleeding and ulceration (all forms), hemorrhoids, hepatic dysfunction (I.V.), hepatic failure, hiatal hernia, ileus (I.V.), indigestion, melena, nausea, necrotizing enterocolitis (I.V.), pancreatitis, peptic ulcer, perforation of stomach or intestine, stomatitis, vomiting (all forms)
GU: Acute renal falure, hematuria, interstitial nephritis, nephrotic syndrome, oliguria (I.V.), proteinuria, renal dysfunction (I.V.), vaginal bleeding
HEME: Agranulocytosis, anemia, aplastic anemia, bone marrow depression, disseminated intravascular coagulation, hemolytic anemia, iron deficiency anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia, unusual bleeding or bruising (all forms)
RESP: Asthma, respiratory depression
SKIN: Ecchymosis, erythema multiforme, erythema nodosum, photosensitivity, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, hyperkalemia (I.V.), hyponatremia (I.V.), injection site irritation

Cautions

Use indomethacin with extreme caution in patients with history of ulcer disease or GI indomethacin 531 G H I bleeding because NSAIDs such as indomethacin increase risk of GI bleeding and ulceration. Expect to use drug for shortest time possible in these patients.

Be aware that serious GI tract ulceration, bleeding, and perforation may occur without
WARNING symptoms. Elderly patients are at greater risk. To minimize risk, give oral indomethacin with food, a full glass of water (not suspension), or an antacid to reduce GI distress.

If GI distress occurs, withhold drug and notify prescriber immediately.

Use indomethacin cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.

Shake suspension well before giving it.

For arthritis, give up to 100 mg of daily dose (not capsules) at bedtime to reduce nighttime pain and morning stiffness.

Make sure suppository stays in rectum at least 1 hour to improve absorption.

To reconstitute I.V. form, add 1 to 2 ml of preservative-free sodium chloride for injection or preservative-free sterile water to vial. Solution made with 1 ml diluent contains 100 mcg (0.1 mg) indomethacin/0.1 ml. Solution made with 2 ml diluent contains 50 mcg (0.05 mg) indomethacin/0.1 ml. Use solution immediately because it contains no preservatives. Discard unused portion.

Be aware that scheduled I.V. doses may be withheld if infant or neonate has anuria or a significant decrease in urine output (less than 0.6 ml/kg/hr).

When using I.V. form, avoid extravasation to protect surrounding tissue.

Anticipate a second course (3 more doses) of I.V. indomethacin if patent ductus arteriosus fails to close or reopens. After two courses, surgery may be performed.
WARNING Monitor patient closely for thrombotic events, including MI and stroke, because NSAIDs increase the risk.

Monitor patient—especially if he’s elderly or receiving long-term indomethacin therapy—for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results because, rarely, elevations may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in elderly patients, those taking diuretics or ACE inhibitors, and those with heart failure, impaired renal function, or hepatic dysfunction; drug may cause renal failure.

Monitor CBC for decreased hemoglobin and hematocrit. Drug may worsen anemia.
WARNING If patient has bone marrow suppression or is receiving an antineoplastic drug, monitor laboratory results (including WBC count), and watch for evidence of infection because anti-inflammatory and antipyretic actions of indomethacin may mask signs and symptoms, such as fever and pain.

Assess patient’s skin regularly for signs of rash or other hypersensitivity reaction because indomethacin is an NSAID and may cause serious skin reactions without
WARNING, even in patients with no history of NSAID sensitivity. At first sign of reaction, stop drug and notify prescriber.

Because indomethacin causes sodium retention, monitor weight and blood pressure, especially if patient has hypertension.

When drug is used to treat gouty arthritis, expect its action to peak in 24 to 36 hours and significant swelling to gradually disappear over 3 to 5 days.

Be aware that form shouldn’t be used to treat gouty arthritis.

Expect to use suppositories for patients who can’t swallow oral form.

To evaluate drug effectiveness, assess for reduced pain and inflammation and improved joint mobility.

Expect patient to have intermittent checkups during long-term therapy and an ophthalmologic examination if vision changes.

PATIENT SAFTY

Urge patient to take indomethacin capsules with full glass of water and to avoid lying down for 15 to 30 minutes afterward. This helps prevent drug from lodging in esophagus and causing irritation. Caution patient not to open or crush capsules.

Instruct patient to take drug with food or an antacid to reduce GI distress.

Instruct patient to make sure suppository indomethacin 532 stays in rectum at least 1 hour.

Urge patient to avoid alcohol during indomethacin therapy.

Remind patient that improvement may not occur for 2 to 4 weeks after starting indomethacin and that he should continue taking drug, as prescribed.

Inform breast-feeding patient that indomethacin appears in breast milk and may cause seizures in infants. Urge her to use another feeding method during therapy.

Caution against prolonged sun exposure during therapy.

Urge patient to notify prescriber immediately about changes in vision or hearing, fever, itching, rash, sore throat, swelling in arms or legs, and weight gain.

Stress importance of having ordered laboratory tests and eye examinations during long-term therapy.

Caution pregnant patient not to take NSAIDs such as indomethacin during last trimester because they may cause premature closure of the ductus arteriosus.

Explain that indomethacin may increase risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.

Explain that indomethacin may increase risk of serious adverse GI reactions; stress need to seek immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.

Alert patient to rare but serious skin reactions. Urge him to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity.

Category

Chemical class: Monoclonal antibody
Therapeutic class: Anti-inflammatory

Pregnancy category: C

Indications

To control moderate to severe Crohn’s disease long-term
IV: Adults and children.Induction: 5 mg/kg over 2 hr, repeated 2 and 6 wk after first infusion. Maintenance: 5 mg/kg over 2 hr every 8 wk.
DOSAGE ADJUSTMENT For adults who respond and then lose response, dosage may be increased to 10 mg/kg. To reduce number of draining enterocutaneous and rectovaginal fistulas and to maintain fistula closure in fistulizing Crohn’s disease
IV:
Adults.Induction: 5 mg/kg over 2 hr, repeated 2 and 6 wk after first infusion. Maintenance: 5 mg/kg over 2 hr every 8 wk.
DOSAGE ADJUSTMENT For patients who respond and then lose response, dosage may be increased to 10 mg/kg. To reduce signs and symptoms, to induce and maintain remission and mucosal healing, and to eliminate corticosteroid use in patients with moderately to severely active ulcerative colitis who have had an inadequate response to conventional therapy
IV:
Adults. 5 mg/kg over 2 hr, repeated 2 and 6 wk after infusion. Maintenance: 5 mg/kg over 2 hr every 8 wk. As adjunct to reduce signs and symptoms, inhibit progression of structural damage, and improve physical function in patients with moderate to severe active rheumatoid arthritis
IV:
Adults. 3 mg/kg, with methotrexate, repeated 2 and 6 wk after first infusion and then every 8 wk thereafter. To treat active ankylosing spondylitis
IV:
Adults. 5 mg/kg, repeated 2 and 6 wk after first infusion and then every 6 wk thereafter. To reduce signs and symptoms, inhibit progression of structural damage, and improve physical function in patients with psoriatic arthritis
IV:
Adults. 5 mg/kg, with or without methotrexate, repeated 2 and 6 wk after first infusion and then every 8 wk thereafter. To treat chronic severe plaque psoriasis in patients who are candidates for sysinfliximab 533 G H I temic therapy but those therapies are medically less appropriate
IV:
Adults. 5 mg/kg, repeated 2 and 6 wk after first infusion and every 8 wk thereafter.

Mechanism of Action

Binds with cytokine tumor necrosis factoralpha (TNF-alpha), preventing it from binding with its receptors. As a result, TNFalpha can’t produce proinflammatory cytokines and endothelial permeability. Infiltration of inflammatory cells into inflamed intestine and joints declines.

Incompatibilities

Don’t infuse infliximab in same I.V. line with other or through plasticized polyvinyl chloride infusion equipment or devices.

Contraindications

Breastfeeding; hypersensitivity to infliximab, murine proteins, or their components; moderate or severe Class III or IV heart failure

Interactions

anakinra, etanercept: Increased risk of neutropenia and serious infections

Side Efect

CNS: Chills, dizziness, fatigue, fever, Guillain-Barré syndrome, headache, meningitis, neuritis, numbness, paresthesia, stroke, syncope, tingling
CV: Arrhythmias, chest pain, hypertension, hypotension, MI, myelitis, neuropathies, pericardial effusion, systemic and cutaneous vasculitis, thrombophlebitis
EENT: Oral candidiasis, pharyngitis, rhinitis, sinusitis, visual changes
GI: Abdominal hernia; abdominal pain; acute hepatic failure; cholecystitis; cholestasis; diarrhea; dyspepsia; elevated aminotranferases; GI hemorrhage; hepatitis; hepatotoxicity; ileus; intestinal obstruction, perforation, or stenosis; melena; pancreatitis; nausea; splenic infarction; splenomegaly; vomiting
GU: Kidney infection, renal failure, ureteral obstruction, UTI, vaginal candidiasis, vaginitis
HEME: Anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia
MS: Ankylosing spondylitis, arthralgia, back pain, limb weakness, myalgia, psoriatic arthritis
RESP: Adult respiratory distress syndrome, bronchitis, cough, dyspnea, interstitial lung disease, pneumonia, tuberculosis, respiratory tract infection, wheezing
SKIN: Facial flushing, jaundice, pruritus, psoriasis, rash, urticaria
Other: Antibody formation to infliximab; bacterial, fungal, or viral infection; infusion reaction; lupuslike symptoms; lymphadenopathy; malignancies, such as leukemia and lymphomas, including hepatosplenic T-cell lymphoma; sepsis

Cautions

Infliximab therapy shouldn’t be started in a patient with an active infection, including serious localized infection.

Use with extreme caution if patient has a history of chronic or recurrent infection, known exposure to tuberculosis, an underlying condition that predisposes to infection, or residence or travel to areas of endemic tuberculosis or mycoses, such as histoplasmosis, coccidioidomycosis, or blastomycosis.

Use cautiously in elderly patients because they have a higher risk of infection.

Use cautiously in patients with previous or ongoing hematologic abnormalities because infliximab may cause serious or even life-threatening adverse hematologic effects. Montior patient’s CBC regularly, as ordered. If adverse effects occur, expect drug to be discontinued.
WARNING Because drug increases risk of developing tuberculosis or reactivating latent tuberculosis, expect prescriber to evaluate patient’s risk and start tuberculosis treatment, as needed, before starting infliximab.
WARNING Infliximab increases risk of serious or fatal opportunistic infections, including invasive fungal infections as well as bacterial and viral infections. The most common ones include aspergillosis, candidiasis, coccidioidomycosis, histoplasmosis, listeriosis, and pneumocytosis.
WARNING Watch for infection, especially if patient receives immunosuppressant therapy or has a chronic infection. Upper resinfliximab 534 piratory tract infections and UTI are most common, but sepsis and fatal infections have occurred.

To reconstitute infliximab, use 21G (or smaller) needle to add 10 ml sterile water for injection to each vial of drug. Swirl to mix; don’t shake. Solution may foam and be clear or light yellow.

Withdraw volume equal to amount of reconstituted drug from a 250-ml glass bottle or polypropylene or polyolefin infusion bag of normal saline solution. Then add reconstituted infliximab to bottle to dilute to 250 ml. Use within 3 hours.

Infuse over at least 2 hours using polyethylene-lined infusion set and in-line, sterile, nonpyrogenic, low–protein-binding filter with pores 1.2 microns or less. Don’t reuse.

Be prepared to stop infusion if hypersensitivity or CNS reaction occurs. Keep acetaminophen, antihistamines, corticosteroids, and epinephrine on hand. A reaction may occur 2 hours to 12 days after infusion.
WARNING Avoid giving drug to patients with New York Heart Association Class III or IV congestive heart failure (CHF) because it may worsen the condition or cause death. If patient does receive infliximab, expect to stop it if CHF worsens.

Because severe hepatic reactions may occur, monitor liver function. Expect to stop drug if jaundice develops or liver enzymes are 5 times or more the upper limit of normal.

Be aware that infliximab is a tumor necrosis factor (TNF) blocker. Malignancies, especially leukemia and such rare lymphomas as hepatosplenic T-cell lymphoma have been reported in patients, particularly children and adolescents, receiving TNF blockers. Patients at increased risk of leukemia are those with rheumatoid arthritis. Patients at increased risk of lymphomas are those with rheumatoid arthritis, Crohn’s disease, ankylosing spondylitis, psoriatic arthritis, and plaque psoriasis, especially those with long-term or very active disease. Monitor them closely.

PATIENT SAFTY

Inform patient that infliximab should take effect within 1 to 2 weeks.

Urge patient to report evidence of infection, such as painful urination, cough, and sore throat. Infusion reaction (chest pain, chills, dyspnea, facial flushing, fever, itching, headache, rash) may occur for up to 12 days.

Explain that infliximab increases the risk of lymphoma; urge prompt medical attention for suspicious signs or symptoms.

Category

Chemical class: Cephaelis acuminata or Cephaelis ipecacuanha derivative
Therapeutic class: Emetic

Pregnancy category: C

Indications

To induce vomiting after drug overdose and certain types of poisoning SYRUP Adults and children over age 12.15 to 30 ml followed by 240 ml water. Dose repeated if vomiting doesn’t begin within 20 to 30 min. Children ages 1 to 12. 15 ml preceded or followed by 120 to 240 ml water. Dose repeated if vomiting doesn’t begin within 20 to 30 min. Infants ages 6 months to 1 year. 5 to 10 ml preceded or followed by 120 to 240 ml water. Route Onset Peak Duration P.O. 20–30 min Unknown 20–25 min

Mechanism of Action

Induces vomiting by irritating gastric mucosa and stimulating medullary chemoreceptor trigger zone in CNS.

Contraindications

Loss of gag reflex, poisoning with strychnine or corrosives (such as alkaloid substances, petroleum distillates, and strong acids), seizures, semiconsciousness or unconsciousness, severe inebriation, shock

Interactions

activated charcoal: Lack of emetic effect

Side Efect

CNS: Depression, drowsiness
EENT: Aspiration of vomitus, coughing
GI: Diarrhea, indigestion ipecac syrup 535 G H I

Cautions

Give ipecac syrup only to conscious patients, and follow with adequate water. Give young or frightened children water before or after ipecac.

Expect vomiting to start in 20 to 30 minutes.

If vomiting doesn’t start within 30 minutes of second dose, prepare for gastric lavage.

Don’t give ipecac after ingestion of petroleum distillates, such as gasoline, or caustic substances, to avoid further injury to esophagus.

If activated charcoal will be given, expect to do so after patient vomits or 30 minutes after second ipecac dose because activated charcoal adsorbs and inhibits ipecac.

Arrhythmias, atrial fibrillation, bradycardia, fatal myocarditis, hypotension, myalgia, or muscle stiffness or weakness may develop if patient takes too much ipecac or doesn’t vomit.

PATIENT SAFTY

Inform patient of ipecac’s effects.

Tell adult patient to drink 8 oz (240 ml) of water after taking drug and child to drink 4 to 8 oz (120 to 240 ml) before or after taking drug.

Inform patient or parents of child that diarrhea may occur after taking drug.

Urge parents to keep ipecac syrup and phone number of a poison control center.
WARNING Advise parents to replace their ipecac extract or tincture with ipecac syrup. Explain that ipecac fluid extract is 14 times more concentrated than ipecac syrup and can cause serious, possibly toxic, effects if given incorrectly.

Category

Chemical class: Quaternary N-methyl isopropyl derivative of noratropine
Therapeutic class: Anticholinergic, bronchodilator

Pregnancy category: B

Indications

To treat bronchitis and COPD INHALATION AEROSOL Adults and adolescents.2 to 4 inhalations (36 to 72 mcg) t.i.d. or q.i.d. Maximum: Up to 12 inhalations (216 mcg)/24 hr. INHALATION SOLUTION FOR NEBULIZER Adults and adolescents. 250 to 500 mcg dissolved in preservative-free sterile normal saline solution every 6 to 8 hr. For severe COPD exacerbations, 500 mcg every 4 to 8 hr. To treat perennial and allergic rhinitis
NASAL SPRAY Adults and children age 6 and over. 2 sprays of 0.03% (21 mcg/spray) per nostril b.i.d. or t.i.d. Maximum: 12 sprays (252 mcg)/ 24 hr. To treat rhinorrhea caused by the common cold
NASAL SPRAY Adults and children age 5 and over. 2 sprays of 0.06% (42 mcg/spray) per nostril t.i.d. or q.i.d. for up to 4 days. Maximum: 16 sprays (672 mcg)/24 hr. Route Onset Peak Duration Inhalation 5–15 min 1–2 hr 3–8 hr Nasal 5 min 1–4 hr 4–8 hr

Contraindications

Hypersensitivity to atropine, ipratropium bromide, or their components; hypersensitivity to peanuts, soya lecithin, soybeans, or related products (with aerosol inhaler)

Interactions

anticholinergics: Increased anticholinergic effects tacrine: Decreased effects of both

Side Efect

CNS: Dizziness, insomnia
CV: Atrial fibrillation (oral inhalation), bradycardia (
NASAL SPRAY), edema, hypertension, palpitations, supraventricular tachycardia (oral inhalation), tachycardia
EENT: Acute eye pain, dry mouth or pharyngeal area, laryngospasm, taste perversion (all drug forms); blurred vision, eye irritation and pain, glaucoma or worsening of existing glaucoma (if
NASAL SPRAY comes in contact with eyes); epistaxis, mydriasis, nasal dryness and irritation, pharyngitis, ipratropium bromide 536 rhinitis, sinusitis, tinnitus (with
NASAL SPRAY)
GI: Bowel obstruction, constipation, diarrhea, ileus, nausea, vomiting
GU: Prostatitis, urine retention
MS: Arthritis
RESP: Bronchitis, bronchospasm, cough, dyspnea, increased sputum production, wheezing
SKIN: Dermatitis, pruritus, rash, urticaria
Other: Anaphylaxis, angioedema, flulike symptoms

Cautions

Use ipratropium cautiously in patients with angle-closure glaucoma, benign prostatic hyperplasia, or bladder neck obstruction and in patients with hepatic or renal dysfunction.

As prescribed, mix ipratropium inhalation solution with preservative-free albuterol, and preservative-free ipratropium inhalation solution with cromolyn inhalation solution. Use within 1 hour.

When using a nebulizer, apply a mouthpiece to prevent drug from leaking out around mask and causing blurred vision or eye pain.

PATIENT SAFTY

Caution patient not to use ipratropium to treat acute bronchospasm.

Inform patient that although some people feel relief within 24 hours of drug use, maximum effect may take up to 2 weeks.

Teach patient to use inhaler or
NASAL SPRAY. Tell him to shake inhaler well at each use.

Advise patient to keep spray out of his eyes because it may irritate them or blur his vision. If spray comes in contact with eyes, instruct patient to flush them with cool tap water for several minutes and to contact prescriber.

Instruct patient to rinse mouth after each nebulizer or inhaler treatment to help minimize throat dryness and irritation.

If patient is using 0.06%
NASAL SPRAY for a common cold, advise against use for longer than 4 days.

Teach patient to track canister contents by counting and recording number of doses.

Advise patient to report decreased response to ipratropium as well as difficulty voiding, eye pain, nasal dryness, nose bleeds, palpitations, and vision changes.

Category

Chemical class: Nonpeptide angiotensin II antagonist
Therapeutic class: Antihypertensive

Pregnancy category: D

Indications

To manage hypertension, alone or with other antihypertensives irbesartan 537 G H I Cholinergic fiber Muscarinic receptor Acetylcholine Ipratropium Smooth-muscle cell membrane

Mechanism of Action

After acetylcholine is released from cholinergic fibers, ipratropium prevents it from attaching to muscarinic receptors on membranes of smooth-muscle cells, as shown at right. By blocking acetycholine’s effects in bronchi and bronchioles, ipratropium relaxes smooth muscles and causes bronchodilation. Adults and adolescents.Initial: 150 mg daily. Maximum: 300 mg daily.
DOSAGE ADJUSTMENT Initial dosage reduced to 75 mg daily for patients with hypovolemia or hyponatremia from such causes as hemodialysis or vigorous diuretic therapy. Children ages 6 to 12. Initial: 75 mg daily. Maximum: 150 mg daily. To treat nephropathy in type 2 diabetes mellitus
Adults. 300 mg daily. Route Onset Peak Duration P.O. Unknown In 4–6 wk Unknown

Mechanism of Action

Selectively blocks binding of the potent vasoconstrictor angiotensin (AT) II to AT1 receptor sites in many tissues, including vascular smooth muscle and adrenal glands. This inhibits the vasoconstrictive and aldosterone-secreting effects of AT II, which reduces blood pressure.

Contraindications

Hypersensitivity to irbesartan or its components

Interactions

diuretics: Possibly additive hypotensive effects

Side Efect

CNS: Anxiety, dizziness, fatigue, headache, nervousness
CV: Chest pain, hypotension, peripheral edema, tachycardia
EENT: Pharyngitis, rhinitis
GI: Abdominal pain, diarrhea, heartburn, hepatitis, indigestion, nausea, vomiting
GU: UTI
MS: Musculoskeletal pain
RESP: Upper respiratory tract infection
SKIN: Rash

Cautions

If patient has known or suspected hypovolemia,provide treatment,such as I.V.normal saline solution,as prescribed,to correct this condition before beginning irbesartan therapy.Or expect to begin therapy with a lower dosage.

Check blood pressure often to evaluate drug’s effectiveness.

If blood pressure isn’t controlled with irbesartan alone, expect to also give a diuretic, such as hydrochlorothiazide, as prescribed.
WARNING If patient receives a diuretic or another antihypertensive during irbesartan therapy, frequently monitor blood pressure because he’s at risk for hypotension.

If patient experiences symptomatic hypotension, expect to stop drug temporarily. Immediately place him in supine position and prepare to give I.V. normal saline solution, as prescribed. Expect to resume drug therapy after blood pressure stabilizes.

If patient receives a diuretic, provide adequate hydration, as appropriate, to help prevent hypovolemia. Also monitor patient for signs and symptoms of hypovolemia, such as hypotension, dizziness, and fainting.
WARNING Monitor patient for increased BUN and serum creatinine levels if he has heart failure or impaired renal function because drug may cause acute renal failure. If increases are significant or persistent, notify prescriber immediately.

PATIENT SAFTY

Advise patient to take drug at the same time each day to maintain its therapeutic effect.

Explain importance of regular exercise, proper diet, and other lifestyle changes in controlling hypertension.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to consult prescriber before taking any new drug.

To reduce risk of dehydration and hypotension, advise patient to drink adequate fluids during hot weather and exercise.

Instruct patient to contact prescriber if severe nausea, vomiting, or diarrhea occurs and continues because of the risk of dehydration and hypotension.

Advise female patient to notify prescriber immediately about known or suspected pregnancy. Explain that if she becomes pregnant, prescriber may replace irbesartan with another antihypertensive that’s safe to use during pregnancy.

Urge patient to keep follow-up appointments with prescriber to monitor progress.

Category

Chemical class: Iron salt, mineral
Therapeutic class: Antianemic

Pregnancy category: C

Indications

To treat iron deficiency anemia
IV: Adults and children weighing more than 15 kg (33 lb). Dose (ml) 5 0.0442 (desired hemoglobin 2 observed hemoglobin) 3 lean body weight (kg) 1 (0.26 3 lean body weight). Or, consult dosage table in package insert. Maximum: 2 ml (100 mg) daily. Children over age 4 months weighing 5 to 15 kg (11 to 33 lb). Dose (ml) 5 0.0442 (desired hemoglobin 2 observed hemoglobin) 3 weight (kg) 1 (0.26 3 weight). Or, consult dosage table in package insert. Maximum: 1 ml (50 mg) daily. To replace iron lost in blood loss
IV:
Adults. Replacement iron (mg) 5 ml of blood loss 3 hematocrit.

Mechanism of Action

Restores hemoglobin and replenishes iron stores. Iron, an essential component of hemoglobin, myoglobin, and several enzymes (including cytochromes, catalase, and peroxidase), is needed for catecholamine metabolism and normal neutrophil function. In iron dextran therapy, iron binds to available protein parts after the drug has been split into iron and dextran by cells of the reticuloendothelial system. The bound iron forms hemosiderin or ferritin, physiologic forms of iron, and transferrin, which replenish hemoglobin and depleted iron stores. Dextran is metabolized or excreted.

Incompatibilities

Don’t mix iron dextran with blood for transfusion, other , or parenteral nutrition solutions for I.V. infusion.

Contraindications

Anemia other than iron deficiency, hypersensitivity to iron dextran or its components

Side Efect

CNS: Chills, disorientation, dizziness, fever, headache, malaise, paresthesia, seizures, syncope, unconsciousness, weakness
CV: Arrhythmias, bradycardia, chest pain, hypertension, hypotension, shock, tachycardia
EENT: Altered taste
GI: Abdominal pain, diarrhea, nausea, vomiting
GU: Hematuria
HEME: Leukocytosis
MS: Arthralgia, arthritis, backache, myalgia, rhabdomyolysis
RESP: Bronchospasm, dyspnea, respiratory arrest, wheezing
SKIN: Cyanosis, diaphoresis, rash, pruritus, purpura, urticaria
Other: Anaphylaxis, infusion site phlebitis

Cautions

Expect oral iron therapy to stop before iron dextran therapy starts. Iron dextran is given only when oral therapy isn’t feasible; it also may be given by I.M. injection.

Expect to monitor hemoglobin level, hematocrit, serum ferritin level, and transferrin saturation, as ordered, before, during, and after iron dextran therapy.
WARNING Before starting iron dextran therapy, give a test dose of 0.5 ml iron dextran gradually over 30 seconds, as prescribed, and monitor patient closely for anaphylactic reaction.

Wait 1 to 2 hours before giving remainder of dose. Infuse undiluted iron dextran slowly, at no more than 1 ml/minute (50 mg/minute).
WARNING Monitor patient closely for signs and symptoms of anaphylaxis (such as severe hypotension, loss of consciousness, collapse, dyspnea, and seizures) during and after infusion. Patients with a history of asthma or allergies are at increased risk for anaphylaxis, possibly death. Institute emergency resuscitation measures as needed, including epinephrine administration, as prescribed.
WARNING Assess blood pressure often after iron dextran administration because hypotension is a common adverse effect that may be related to infusion rate; avoid rapid infusion. iron dextran 539 G H I

Be aware that patient may have adverse reactions, including arthralgia, backache, chills, and vomiting, 1 to 2 days after drug therapy. Symptoms should resolve within 3 to 4 days.

Assess patients with a history of rheumatoid arthritis for exacerbation of joint pain and swelling.

If patient has cardiovascular disease, watch for worsening from drug’s adverse effects.

Assess patient for iron overload, characterized by sedation, decreased activity, pale eyes, and bleeding in GI tract and lungs.

Store iron dextran at 59° to 86° F (15° to 30° C ).

PATIENT SAFTY

Instruct patient to immediately report signs of adverse reaction, such as shortness of breath, wheezing, or rash, during iron dextran therapy.

Advise patient not to take any oral iron without first consulting prescriber.

Inform patient that symptoms of iron deficiency may include decreased stamina, learning problems, shortness of breath, and fatigue. Urge patient to plan periods of activity and rest to avoid excessive fatigue.

Stress need to follow dosage regimen and keep follow-up medical and laboratory appointments.

Category

Chemical class: Iron salt, mineral
Therapeutic class: Antianemic

Pregnancy category: B

Indications

To treat iron deficiency anemia in hemodialysis patients receiving erythropoietin
I.V.INJECTION
Adults. Initial: 100 mg elemental iron injected undiluted over 2 to 5 min during dialysis. Usual: 100 mg elemental iron every wk to 3 times/wk to total dose of 1,000 mg. Dosage repeated as needed to maintain target levels of hemoglobin and hematocrit and acceptable blood iron level. Maximum: 100 mg/dose.
IV:
Adults. Initial: 100 mg elemental iron infused diluted over 15 min during dialysis. Usual: 100 mg elemental iron every wk to 3 times/wk to a total dose of 1,000 mg. Dosage repeated as needed to maintain target levels of hemoglobin and hematocrit and acceptable blood iron level. Maximum: 100 mg/dose. To treat iron deficiency anemia in peritoneal dialysis patients receiving erythropoietin
IV:
Adults. Initial: 300 mg elemental iron infused diluted over 1.5 hr on days 1 and 14, followed by 400 mg elemental iron infused over 2.5 hr on day 28. Dosage repeated as needed to maintain target levels of hemoglobin and hematocrit and acceptable blood iron level. Maximum: 1,000 mg/ 28 days. To treat iron deficiency anemia in nondialysis patients with chronic renal disease regardless of whether they’re receiving erythropoietin
I.V.INJECTION
Adults. Initial: 200 mg elemental iron injected undiluted over 2 to 5 min and repeated 4 more times over a 14-day period for a total dose of 1,000 mg. Dosage repeated as needed to maintain target levels of hemoglobin and hematocrit and acceptable blood iron level. Maximum: 1,000 mg/ 14 days.
IV:
Adults.500 mg elemental iron infused diluted over 3.5 to 5 hr on days 1 and 14. Dosage repeated as needed to maintain target levels of hemoglobin and hematocrit and acceptable blood iron level. Maximum: 1,000 mg/14 days.

Mechanism of Action

Acts to replenish iron stores lost during dialysis because of increased erythropoiesis and insufficient absorption of iron from GI tract. Iron is an essential component of hemoglobin, myoglobin, and several enzymes, including cytochromes, catalase, and peroxidase, and is needed for catecholamine metabolism and normal neuiron sucrose 540 trophil function. Iron sucrose injection also normalizes RBC production by binding with hemoglobin or being stored as ferritin in reticuloendothelial cells of the liver, spleen, and bone marrow.

Incompatibilities

Don’t mix with other or parenteral nutrition solutions for I.V. infusion.

Contraindications

Anemia other than iron deficiency, hypersensitivity to iron salts or their components, iron overload

Interactions

chloramphenicol: Possibly decreased effectiveness of iron sucrose oral iron preparations: Possibly reduced absorption of oral iron supplements

Side Efect

CNS: Asthenia, dizziness, fatigue, fever, headache, hypoesthesia, malaise
CV: Chest pain, heart failure, hypertension, hypotension, peirpheral edema
EENT: Conjunctivitis, ear pain, nasal congestion, nasopharyngitis, rhinitis, sinusitis, taste perversion
ENDO: Hyperglycemia, hypoglycemia
GI: Abdominal pain, constipation, diarrhea, elevated liver function test results, nausea, occult-positive feces, peritoneal infection, vomiting
GU: UTI
MS: Arthralgia, arthritis, back pain, leg cramps, muscle pain or weakness, myalgia
RESP: Cough, dyspnea, pneumonia, upper respiratory tract infection
SKIN: Pruritus, rash
Other: Anaphylaxis; fluid overload; gout; hypervolemia; infusion or injection site burning, pain, or redness; sepsis

Cautions

To reconstitute iron sucrose injection for infusion, dilute 100 mg elemental iron in maximum of 100 ml normal saline solution (for hemodialysis patients) or 250 ml (for peritoneal dialysis and nondialysis patients) immediately before infusion. Discard any unused diluted solution.

Give drug directly into dialysis line by slow I.V. injection or by infusion.
WARNING Monitor patient closely for evidence of anaphylaxis, such as severe hypotension, loss of consciousness, collapse, dyspnea, or seizures, during and after therapy. Institute emergency resuscitation measures as needed.
WARNING Assess blood pressure often after drug administration because hypotension is a common adverse reaction that may be related to infusion rate (avoid rapid infusion) or total cumulative dose.

Monitor hemoglobin, hematocrit, serum ferritin, and transferrin saturation, as ordered, before, during, and after iron sucrose therapy. Test serum iron level 48 hours after last dose. Notify prescriber and expect to stop therapy if blood iron levels are normal or elevated, to prevent iron toxicity.

Watch for evidence of iron overload, such as sedation, decreased activity, pale eyes, and bleeding in GI tract and lungs.

PATIENT SAFTY

Advise patient not to take any oral iron preparations during iron sucrose therapy without first consulting prescriber.

Inform patient that symptoms of iron deficiency may include decreased stamina, learning problems, shortness of breath, and fatigue.

Category

Chemical class: Hydrazine derivative
Therapeutic class: Antidepressant

Pregnancy category: C

Indications

To treat major depression Adults and adolescents over age 16. Initial: 10 mg b.i.d., increased by 10 mg daily every 2 to 4 days, as needed and tolerated. Maximum: 60 mg daily. Route Onset Peak Duration P.O. 7–10 days Unknown 10 days

Mechanism of Action

Irreversibly binds to MAO, reducing its activity and increasing levels of neurotransisocarboxazid 541 G H I mitters, including serotonin and the catecholamine neurotransmitters dopamine, epinephrine, and norepinephrine. This regulation of CNS neurotransmitters helps to ease depression. With long-term use, drug results in down-regulation (desensitization) of alpha2or beta-adrenergic and serotonin receptors after 2 to 4 weeks, which also produces an antidepressant effect.

Contraindications

Cardiovascular disease; cerebrovascular disease; heart failure; hepatic disease; history of headaches; hypersensitivity to isocarboxazid or its components; hypertension; pheochromocytoma; severe renal impairment; use of anesthetics, antihypertensives, bupropion, buspirone, carbamazepine, CNS depressants, cyclobenzaprine, dextromethorphan, meperidine, selective serotonin reuptake inhibitors, sympathomimetics, or tricyclic antidepressants; use within 14 days of another MAO inhibitor

Interactions

anticholinergics, antidyskinetics, antihistamines: Increased anticholinergic effect, prolonged CNS depression (with antihistamines) anticonvulsants: Increased CNS depression, possibly altered seizure pattern antihypertensives, diuretics: Increased hypotensive effect bromocriptine: Possibly interference with bromocriptine effects
bupropion: Increased risk of bupropion toxicity buspirone, guanadrel, guanethidine: Increased risk of hypertension caffeine-containing : Increased risk of dangerous arrhythmias and severe hypertension carbamazepine, cyclobenzaprine, maprotiline, other
MAO inhibitors: Increased risk of hyperpyretic crisis, hypertensive crisis, severe seizures, and death; altered pattern of seizures (with carbamazepine)
CNS depressants: Increased CNS depression dextromethorphan: Increased risk of excitation, hypertension, and hyperpyrexia doxapram: Increased vasopressor effects of either drug fluoxetine, paroxetine, sertraline, trazodone, tricyclic antidepressants: Increased risk of life-threatening serotonin syndrome haloperidol, loxapine, molindone, phenothiazines, pimozide,
thioxanthenes: Prolonged and intensified anticholinergic, hypotensive, and sedative effects insulin, oral antidiabetic : Increased hypoglycemic effects levodopa: Increased risk of sudden, moderate to severe hypertension local anesthetics (with epinephrine or levonordefrin): Possibly severe hypertension meperidine, other opioid analgesics: Increased risk of coma, hyperpyrexia, hypotension, immediate excitation, rigidity, seizures, severe hypertension, severe respiratory depression, shock, sweating, and death methyldopa: Increased risk of hallucinations, headache, hyperexcitability, and severe hypertension
methylphenidate: Increased CNS stimulation metrizamide: Decreased seizure threshold and increased risk of seizures oral anticoagulants: Increased anticoagulant activity phenylephrine (nasal or ophthalmic): Potentiated vasopressor effect of phenylephrine rauwolfia alkaloids: Increased risk of moderate to severe hypertension, CNS depression (when isocarboxazid is added to rauwolfia alkaloid therapy), CNS excitation and hypertension (when rauwolfia alkaloid is added to isocarboxazid therapy) spinal anesthetics: Increased risk of hypotension sympathomimetics: Prolonged and intensified cardiac stimulant and vasopressor effects tryptophan: Increased risk of confusion, disorientation, hyperreflexia, hyperthermia, hyperventilation, mania or hypomania, and shivering aged cheese; avocados; bananas; fava or broad beans; cured meat or sausage; overripe fruit; pickled or smoked fish, meats or poultry; protein extract; soy sauce; yeast extract; and other high in tyramine or other pressor amines: Increased risk of dangerous arrhythmias and severe hypertensive crisis alcohol-containing products that also may contain tyramine, such as beer (including isocarboxazid 542 reduced-alcohol and alcohol-free beer), hard liquor, liqueurs, sherry, and wines (red and white): Increased risk of developing hypertensive crisis

Side Efect

CNS: Agitation, dizziness, drowsiness, fever, headache, insomnia, intracranial bleeding, overstimulation, restlessness, sedation, suicidal ideation, tremor, weakness
CV: Bradycardia, chest pain, edema, hypertensive crisis, orthostatic hypotension, palpitations, tachycardia
EENT: Blurred vision, dry mouth, mydriasis, photophobia, yellowing of sclera
GI: Abdominal pain, anorexia, constipation, diarrhea, elevated liver function test results, increased appetite, nausea
GU: Dark urine, oliguria, sexual dysfunction
HEME: Leukopenia
MS: Muscle spasms, myoclonus, neck stiffness
SKIN: Clammy skin, diaphoresis, jaundice, rash
Other: Unusual weight gain

Cautions

Monitor patient’s blood pressure during isocarboxazid therapy to detect hypertensive crisis and decrease risk of orthostatic hypotension.
WARNING Notify prescriber immediately if patient has evidence of hypertensive crisis (drug’s most serious adverse effect), such as chest pain, headache, neck stiffness, and palpitations. Expect to stop drug immediately if these occur.

Keep phentolamine readily available to treat hypertensive crisis. Give 5 mg by slow I.V. infusion, as prescribed, to reduce blood pressure without causing excessive hypotension. Use external cooling measures, as prescribed, to manage fever.

To avoid hypertensive crisis, expect to wait 10 to 14 days when switching patient from one MAO inhibitor to another or when switching from a dibenzazepine-related drug,such as amitriptyline or perphenazine.

Monitor patient with a history of epilepsy for seizures because isocarboxazid may alter seizure threshold. Institute seizure precautions according to facility protocol.

Monitor liver function test results, and assess patient for abdominal pain, dark urine, and jaundice because isocarboxazid may cause hepatic dysfunction.

Expect to observe some therapeutic effect in 7 to 10 days, but keep in mind that full effect may not occur for 4 to 8 weeks.

Be aware that, for maintenance therapy, the smallest possible dose should be used. Once clinical effect has been achieved, expect to decrease the dosage slowly over several weeks.

Keep dietary restrictions in place for at least 2 weeks after stopping isocarboxazid because of slow recovery from drug’s enzyme-inhibiting effects.

Ideally, expect to stop drug 10 days before elective surgery, as prescribed, to avoid hypotension.

Anticipate that coadministration with a selective serotonin reuptake inhibitor may cause confusion, diaphoresis, diarrhea, seizures, and other less severe symptoms.

Monitor depressed patient for suicidal tendencies, especially when therapy starts or dosage changes, because depression may worsen temporarily. If suicidal tendencies arise, institute suicide precautions, as appropriate and according to facility policy, and notify prescriber immediately.

Monitor patient for sudden insomnia. If it develops, notify prescriber and be prepared to give drug early in the day.

PATIENT SAFTY

Inform patient and family members that therapeutic effects of isocarboxazid may take several weeks to appear and that he should continue taking drug as prescribed.

Caution parents to monitor pediatric patients, including adolescents, closely for suicidal tendencies, especially when therapy starts or dosage changes.

Caution patient to rise slowly from a lying or sitting position to minimize effects of orthostatic hypotension.
WARNING Instruct patient to avoid the following , beverages, and during isocarboxazid therapy and for 2 weeks afterward: alcohol-free and reducedalcohol beer and wine; appetite suppressants; beer; broad beans; cheese (except cottage and cream cheese); chocolate and caffeine in large quantities; dry sausage (including Genoa salami, hard salami, Lebanon bologna, and pepperoni); hay fever ; inhaled asthma ; liver; isocarboxazid 543 G H I meat extract; OTC cold and cough medicines (including those containing dextromethorphan); nasal decongestants (tablets, drops, or spray); pickled herring; products that contain tyramine; protein-rich that may have undergone protein changes by aging, fermenting, pickling, or smoking; sauerkraut; sinus ; weight-loss products; yeast extracts (including brewer’s yeast in large quantities); yogurt; and wine.

Advise patient to notify prescriber immediately about chest pain, dizziness, headache, nausea, neck stiffness, palpitations, rapid heart rate, sweating, and vomiting.

Advise patient to inform all health care providers (including dentists) that he takes an MAO inhibitor because certain are contraindicated within 2 weeks of it.

Urge patient to avoid hazardous activities until drug’s adverse effects are known.

Urge patient with diabetes mellitus who’s taking insulin or an oral antidiabetic to check blood glucose level often during therapy because isocarboxazid may affect glucose control.

Caution patient not to stop taking drug abruptly to avoid recurrence of original symptoms.

Category

Chemical class: Catecholamine
Therapeutic class: Bronchodilator

Pregnancy category: Not rated

Indications

To prevent and treat reversible bronchospasm from chronic bronchitis or emphysema INHALATION AEROSOL Adults and adolescents. 1 or 2 inhalations (340 or 680 mcg) every 4 hr. INHALATION SOLUTION FOR HAND-BULB NEBULIZER
Adults.3 to 7 inhalations of undiluted 0.5% or 1% solution every 4 hr. INHALATION SOLUTION FOR NEBULIZER
Adults. 2.5 to 10 mg over 15 to 20 min. Repeated every 4 hr, p.r.n. Route Onset Peak Duration Inhalation 5 min 5–15 min 2–3 hr

Mechanism of Action

Attaches to beta2receptors on bronchial cell membranes, which stimulates the intracellular enzyme adenylate cyclase to convert adenosine triphosphate to cyclic adenosine monophosphate (cAMP). Increased intracellular levels of cAMP help relax bronchial smooth-muscle cells, stabilize mast cells, and inhibit histamine release.

Contraindications

Hypersensitivity to isoetharine, sympathomimetic amines, or their components

Interactions

beta blockers: Decreased effects of both cyclopropane, halothane: Increased risk of arrhythmias ephedrine: Increased cardiac stimulation epinephrine: Increased epinephrine effects guanethidine: Decreased hypotensive effects isoproterenol: Excessive cardiac stimulation
MAO inhibitors: Increased risk of hypertensive crisis, increased vascular effects of isoetharine methyldopa: Increased vasopressor response nitrates: Possibly decreased effects of both oxytocic : Increased risk of hypotension rauwolfia alkaloids: Increased risk of hypertension tricyclic antidepressants: Increased risk of arrhythmias

Side Efect

CNS: Anxiety, dizziness, headache, insomnia, tremor, vertigo, weakness
CV: Angina, arrhythmias, hypertension, palpitations, tachycardia isoetharine 544
EENT: Choking sensation, eyelid or lip swelling, laryngospasm, taste perversion
GI: Nausea, vomiting
RESP: Bronchospasm, cough, paradoxical increased airway resistance (with excessive use), wheezing
SKIN: Dermatitis, flushing, pruritus, urticaria
Other: Angioedema, facial edema

Cautions

Dilute 1% isoetharine inhalation solution with 1 to 4 ml sterile normal saline solution; 0.062% to 0.25% solutions don’t need to be diluted before use.

Don’t use a solution that’s pink or darker than light yellow or one that contains precipitate.

Wait 1 minute after initial inhaler dose to assess whether patient needs a second dose.

Monitor blood pressure and pulse, and observe for arrhythmias during therapy.

PATIENT SAFTY

Teach patient how to use isoetharine inhaler or nebulizer.

Instruct patient to take drug exactly as directed and not to exceed dosage.

Instruct patient not to take other , even OTC , unless prescribed.

Teach patient how to determine when canister needs to be replaced by counting and recording number of doses.

Instruct patient to report chest pain, difficulty breathing, failure to respond to usual isoetharine dose, irregular heartbeat, productive cough, or tremor.

Category

Chemical class: Isonicotinic acid derivative
Therapeutic class: Antibiotic, antitubercular

Pregnancy category: C

Indications

To prevent tuberculosis SYRUP,,
I.M.INJECTION Adults and adolescents. 300 mg daily. Children.10 mg/kg daily (up to 300 mg). As adjunct to treat active tuberculosis SYRUP, Adults and adolescents.300 mg daily or 15 mg/kg (up to 900 mg) 2 or 3 times/wk, based on treatment regimen. Children.10 to 20 mg/kg (up to 300 mg) daily or 20 to 40 mg/kg (up to 900 mg) 2 or 3 times/wk, based on treatment regimen.
I.M.INJECTION Adults and adolescents.5 mg/kg (up to 300 mg) daily or 15 mg/kg (up to 900 mg) 2 or 3 times/wk, based on treatment regimen. Children.10 to 20 mg/kg (up to 300 mg) daily or 20 to 40 mg/kg (up to 900 mg) 2 or 3 times/wk, based on treatment regimen.

Mechanism of Action

Interferes with lipid and nucleic acid synthesis in actively growing tubercule bacilli cells. Isoniazid also disrupts bacterial cell wall synthesis and may interfere with mycolic acid synthesis in mycobacterial cells.

Contraindications

History of serious

Side Efect

(such as hepatic injury) from isoniazid, hypersensitivity to isoniazid or its components

Interactions

acetaminophen: Increased risk of hepatotoxicity and possibly nephrotoxicity alfentanil: Decreased alfentanil clearance and increased duration of effects aluminum-containing antacids: Decreased isoniazid absorption benzodiazepines: Decreased benzodiazepine clearance carbamazepine: Increased blood carbamazepine level and toxicity, increased risk of isoniazid toxicity corticosteroids: Decreased isoniazid effects cycloserine: Increased risk of adverse CNS effects and CNS toxicity disulfiram: Changes in behavior and coordination enflurane: Increased risk of high-output renal failure halothane: Increased risk of hepatotoxicity and hepatic encephalopathy hepatotoxic ,
rifampin: Increased risk isoniazid 545 G H I of hepatotoxicity
ketoconazole: Possibly decreased blood ketoconazole level and resistance to antifungal treatment meperidine: Risk of hypotensive episodes or CNS depression nephrotoxic : Increased risk of nephrotoxicity oral anticoagulants: Increased anticoagulation
phenytoin: Increased blood phenytoin level, increased risk of phenytoin toxicity
theophylline: Increased theophylline level histamine-containing , such as tuna, skipjack, and other tropical fish: Inhibited action of the enzyme diamine oxidase in , possibly resulting in headache, sweating, palpitations, flushing, and hypotension. tyramine-containing , such as cheese and fish: Increased response to tyramine in , possibly resulting in chills; diaphoresis; headache; light-headedness; and red, itchy, clammy skin
alcohol use: Increased risk of hepatotoxicity and increased isoniazid metabolism

Side Efect

CNS: Clumsiness, confusion, dizziness, encephalopathy, fatigue, fever, hallucinations, neurotoxicity, paresthesia, peripheral neuritis, psychosis, seizures, weakness
CV: Vasculitis
EENT: Optic neuritis
ENDO: Gynecomastia, hyperglycemia
GI: Abdominal pain, anorexia, elevated liver function test results, epigastric distress, hepatitis, nausea, vomiting
GU: Glycosuria
HEME: Agranulocytosis, aplastic anemia, eosinophilia, hemolytic anemia, sideroblastic anemia, thrombocytopenia
MS: Arthralgia, joint stiffness
SKIN: Jaundice, pruritus, rash
Other: Hypocalcemia, hypophosphatemia, injection site irritation, lupus-like symptoms, lymphadenopathy

Cautions

Administer isoniazid cautiously to diabetic, alcoholic, or malnourished patients and those at risk for peripheral neuritis.

Give drug 1 hour before or 2 hours after meals to promote absorption. If GI distress occurs, give drug with a small amount of food or an antacid that doesn’t contain aluminum 1 hour before or 2 hours after meal.

Monitor liver enzyme studies, which may be ordered monthly, because isoniazid can cause severe (possibly fatal) hepatitis.

About 50% of patients metabolize isoniazid slowly, which may lead to increased toxic effects. Watch for

Side Efect

, such as peripheral neuritis; if they occur, expect to decrease dosage.

Give isoniazid with other antituberculotic , as prescribed, to prevent development of resistant organisms.

Be aware that patients with advanced HIV infection may experience more severe

Side Efect

in greater numbers.

PATIENT SAFTY

Instruct patient to take isoniazid exactly as prescribed and not to stop without first consulting prescriber. Explain that treatment may take months or years.

Direct patient to take drug on an empty stomach 1 hour before or 2 hours after meals. If GI distress occurs, instruct him to take drug with food or an antacid that doesn’t contain aluminum.

Advise patient to report signs of hepatic dysfunction, including dark urine, decreased appetite, fatigue, and jaundice.

Caution patient not to drink alcohol while taking isoniazid because alcohol increases the risk of hepatotoxicity.

Give patient a list of tyramine-containing to avoid when taking isoniazid, such as cheese, fish, salami, red wine, and yeast extracts. Explain that consuming these during isoniazid therapy may cause unpleasant

Side Efect

, such as chills, pounding heartbeat, and sweating.

Tell patient to avoid histamine-containing such as tuna, skipjack, and other tropical fish during therapy to avoid such

Side Efect

as headache, sweating, rapid heartbeat, flushing, and low blood pressure.

Tell patient that he’ll need periodic laboratory tests and physical examinations.

Urge patient to report fever, nausea, numbness and tingling in arms and legs, rash, vision changes, vomiting, and yellowing skin.

Category

Chemical class: Catecholamine
Therapeutic class: Antiarrhythmic, bronchodilator

Pregnancy category: B

(inhalation), C (I.V. infusion)

Indications

To treat bronchospasm in asthma and to prevent and treat bronchospasm in COPD INHALATION AEROSOL(ISOPROTERENOL HYDROCHLORIDE) Adults and adolescents.1 oral inhalation (120 to 131 mcg), repeated in 2 to 5 min. Inhalations repeated every 3 to 4 hr, p.r.n. INHALATION AEROSOL(ISOPROTERENOL SULFATE) Adults and adolescents. 1 oral inhalation (80 mcg), repeated in 2 to 5 min. Inhalations repeated every 4 to 6 hr, p.r.n. INHALATION SOLUTION FOR NEBULIZER(ISOPROTERENOL) Adults and adolescents.2.5 mg diluted and administered over 10 to 20 min. Repeated every 4 hr, p.r.n. Children.0.05 to 0.1 mg/kg (up to 1.25 mg) diluted and administered over 10 to 20 min. Repeated every 4 hr, p.r.n. To manage bronchospasm during anesthesia
I.V.INJECTION(ISOPROTERENOL HYDROCHLORIDE)
Adults.0.01 to 0.02 mg, repeated p.r.n. To treat bradycardia with significant hemodynamic change, such as thirddegree heart block or prolonged QT intervals
IV:(ISOPROTERENOL HYDROCHLORIDE)
Adults.Initial: 2 mcg/min. Titrated according to heart rate, as ordered. Maximum: 10 mcg/min. Route Onset Peak Duration I.V.* Unknown Unknown 1–2 hr I.V. In 5 min Unknown 10 min InhalaIn 5 min 5–15 min In 3 hr tion

Mechanism of Action

Stimulates beta1receptors in the myocardium and cardiac conduction system, resulting in positive inotropic and chronotropic effects. Isoproterenol also shortens AV conduction time and refractory period in patients with AV block. This action increases ventricular rate and halts bradycardia and associated syncope. In addition, isoproterenol attaches to beta2receptors on bronchial cell membranes. This action stimulates the intracellular enzyme adenylate cyclase to convert adenosine triphosphate to cyclic adenosine monophosphate (cAMP). An increased intracellular cAMP level relaxes bronchial smooth-muscle cells, stabilizes mast cells, and inhibits histamine release.

Contraindications

Angina pectoris, heart block or tachycardia from digitalis toxicity, ventricular arrhythmias that require inotropic therapy (I.V. form); hypersensitivity to isoproterenol or its components, such as sulfite in some preparations (inhalation form); tachyarrhythmias (I.V. and inhalation forms)

Interactions

Note: All interactions listed are for I.V. form unless indicated. alpha blockers, other with this action: Possibly decreased peripheral vasoconstricting and hypertensive effects of isoproterenol anesthetics (hydrocarbon inhalation): Increased risk of atrial and ventricular arrhythmias astemizole, cisapride, that prolong QTc interval, terfenadine: Possibly prolonged QTc interval beta blockers (ophthalmic): Decreased effects isoproterenol 547 G H I *For treatment of bronchospasm. For treatment of bradycardia. of isoproterenol, increased risk of bronchospasm, wheezing, decreased pulmonary function, and respiratory failure beta blockers (systemic): Increased risk of bronchospasm, decreased effects of both (including inhaled isoproterenol) digoxin: Increased risk of arrhythmias, hypokalemia, and digitalis toxicity diuretics, other antihypertensives: Possibly decreased antihypertensive effects ergot alkaloids: Increased vasoconstriction and vasopressor effects
MAO inhibitors: Intensified and extended cardiac stimulation and vasopressor effects quinidine, other that affect myocardial reaction to sympathomimetics: Increased risk of arrhythmias
theophylline: Increased risk of cardiotoxicity, decreased blood theophylline level thyroid hormones: Increased effects of both , increased risk of coronary insufficiency in patients with coronary artery disease tricyclic antidepressants: Increased vasopressor response, increased risk of prolonged QTc interval and arrhythmias

Side Efect

CNS: Dizziness, headache, insomnia, nervousness, syncope, tremor, weakness
CV: Angina, arrhythmias, bradycardia, hypertension, hypotension, palpitations, tachycardia, ventricular arrhythmias
EENT: Dry mouth, oropharyngeal edema, taste perversion
ENDO: Hyperglycemia
GI: Heartburn, nausea, vomiting
MS: Muscle spasms and twitching
RESP: Bronchitis, bronchospasm, cough, dyspnea, increased sputum production, pulmonary edema, wheezing
SKIN: Dermatitis, diaphoresis, erythema multiforme, flushing, pallor, pruritus, rash, Stevens-Johnson syndrome, urticaria
Other: Angioedema, hypokalemia

Cautions

Expect to give lowest possible dose of isoproterenol for shortest possible time to minimize tolerance.

Don’t administer I.V. isoproterenol if solution is pink or brown or contains precipitate.

Administer isoproterenol infusion through a large vein, and monitor patient for signs of extravasation.

Monitor blood pressure, cardiac rhythm, central venous pressure, and urine output when giving I.V. drug. Adjust infusion rate to response, as ordered.

Notify prescriber immediately if heart rate increases significantly or exceeds 110 beats/ minute during I.V. infusion.

Know that drug may increase pulse pressure and cause hypotension. Expect to reduce I.V. infusion slowly to decrease risk of hypotension.
WARNING Be aware that drug markedly increases risk of arrhythmias. If an arrhythmia develops, expect to give a cardioselective beta blocker, such as atenolol.

Isoproterenol isn’t used regularly to treat asthma, decreased cardiac output, hypotension, or shock because it increases the risk of arrhythmias, hypotension, and ischemia.
WARNING If drug aggravates a ventilationperfusion problem, expect blood oxygen level to fall even as breathing seems to improve.

PATIENT SAFTY

Instruct patient not to use isoproterenol inhaler more often than prescribed because it may cause cardiac and respiratory problems.

Teach patient to use the inhaler. Provide a spacer, as needed.

Instruct patient to wait 2 to 5 minutes before taking second inhalation.

Advise patient to rinse his mouth after inhalation to remove drug residue and minimize mouth dryness.

Inform patient that saliva may appear pink after inhalation.

If patient uses a corticosteroid inhaler, tell him to take isoproterenol first and wait at least 2 minutes before taking corticosteroid.

Instruct patient to notify prescriber about chest pain, dizziness, hyperglycemic symptoms (such as abdominal cramps, lethargy, nausea, and vomiting), insomnia, irregular heartbeat, palpitations, tremor, and weakness.

Advise patient to also report reduced effectiveness of isoproterenol, increased use of inhaler, and increased symptoms after taking drug.

Category

Chemical class: Organic nitrate
Therapeutic class: Antianginal, vasodilator

Pregnancy category: C

Indications

To treat or prevent angina CHEWABLE
Adults. 5 mg every 2 to 3 hr, p.r.n. (dinitrate).
Adults. 40 to 80 mg every 8 to 12 hr (dinitrate).
Adults.20 to 80 mg every 8 to 12 hr (dinitrate); 30 to 60 mg daily, increased gradually as tolerated to 120 mg daily (mononitrate). S.L.
Adults. 2.5 to 5 mg every 2 to 3 hr, p.r.n. (dinitrate).
Adults.5 to 40 mg every 6 hr, adjusted as needed (dinitrate); 20 mg in 2 doses given 7 hr apart (mononitrate). Route Onset Peak Duration P.O.* 1 hr Unknown 5–6 hr P.O. In 3 min Unknown 30 min– (chewable)* 2 hr P.O. 30 min Unknown 6–8 hr ()* P.O. In 3 min Unknown 2 hr (S.L.)*

Contraindications

Angle-closure glaucoma; cerebral hemorrhage; concurrent use of sildenafil; head trauma; hypersensitivity to isosorbide, other nitrates, or their components; orthostatic hypotension; severe anemia

Interactions

acetylcholine, norepinephrine: Possibly decreased effectiveness of these antihypertensives, calcium channel blockers, opioid analgesics, other vasodilators: Increased risk of orthostatic hypotension aspirin: Increased blood level and pharmaisosorbide 549 G H I Cell exterior Isosorbide Nitrate receptor cGMP Calcium Smooth- muscle cell membrane Nitric oxide Guanylate cyclase Cell interior

Mechanism of Action

Isosorbide may interact with nitrate receptors in vascular smooth-muscle cell membranes. By interacting with receptors’ sulfhydryl groups, drug is reduced to nitric oxide. Nitric oxide activates the enzyme guanylate cyclase, increasing intracellular formation of cyclic guanosine monophosphate (cGMP). An increased cGMP level may relax vascular smooth muscle by forcing calcium out of muscle cells, causing vasodilation. This improves cardiac output by reducing mainly preload but also afterload. *For dinitrate. For mononitrate, onset also is 1 hr; peak and duration are unknown. cologic action of isosorbide sildenafil, tadalafil, vardenafil: Increased risk of hypotension and death sympathomimetics: Increased risk of hypotension, possibly decreased therapeutic effects of isosorbide
alcohol use: Increased risk of orthostatic hypotension

Side Efect

CNS: Agitation, confusion, dizziness, headache, insomnia, restlessness, syncope, vertigo, weakness
CV: Arrhythmias, orthostatic hypotension, palpitations, peripheral edema, tachycardia
EENT: Blurred vision, diplopia (all forms); sublingual burning (S.L. form)
GI: Abdominal pain, diarrhea, indigestion, nausea, vomiting
GU: Dysuria, impotence, urinary frequency
HEME: Hemolytic anemia
MS: Arthralgia, muscle twitching
RESP: Bronchitis, pneumonia, upper respiratory tract infection
SKIN: Diaphoresis, flushing, rash

Cautions

Use isosorbide cautiously in patients with hypovolemia or mild hypotension. Monitor patient for increased hypotension and reduced cardiac output.

Give drug 1 hour before or 2 hours after meals. Give with meals if patient experiences severe headaches or adverse GI reactions.

Know that patient may experience daily headaches from isosorbide’s vasodilating effects. Give acetaminophen, as prescribed, to relieve pain.
WARNING Be aware that stopping drug abruptly may cause angina and increase the risk of MI.

Monitor blood pressure often during isosorbide therapy, especially in elderly patients; drug may cause severe hypotension.

Keep isosorbide protected from heat and light.

PATIENT SAFTY

Teach patient and family to recognize signs and symptoms of angina, including chest pain, fullness, or pressure, which commonly is accompanied by sweating and nausea. Pain may radiate down the left arm or into the neck or jaw. Inform female patients and those with diabetes mellitus or hypertension that they may experience only fatigue and shortness of breath.

Caution patient not to crush or chew isosorbide capsules or tablets or S.L. tablets unless specifically ordered to do so by prescriber.

Instruct patient to place S.L. tablet under tongue and not to swallow it, but to let it dissolve. Explain that moisture in mouth promotes drug absorption and that tingling or burning in the mouth indicates drug effectiveness.

Advise patient to chew chewable tablets well and to keep them in his mouth for 1 to 2 minutes before swallowing to enhance drug absorption.

Instruct patient to take drug before any situation or activity that might precipitate angina.

Advise patient to carry isosorbide with him at all times.

Caution patient that abrupt drug discontinuation may cause angina and increase the risk of MI.

Instruct patient to notify prescriber about blurred vision, fainting, increased angina attacks, rash, and severe or persistent headaches.

Teach patient to reduce the effects of orthostatic hypotension by changing position slowly. Advise him to lie down if he becomes dizzy.

Inform patient that drug commonly causes headache, which typically resolves after a few days of continuous therapy. Suggest that patient take acetaminophen as needed and as prescribed.

Advise patient to avoid potentially hazardous activities until drug’s CNS effects are known.

Urge patient to avoid alcohol consumption.

Instruct patient to store drug in a tightly closed container and protect from light and heat.

Advise male patient with erectile dysfunction to alert prescriber that he is taking isosorbide because sildenafil, tadalafil, and vardenafil can cause fatal reactions when taken with isosorbide.

Category

Chemical class: Retinoid
Therapeutic class: Acne inhibitor

Pregnancy category: X

Indications

To treat severe recalcitrant nodular acne unresponsive to conventional therapy
Adults. Initial: 0.5 mg to 1 mg/kg daily in 2 divided doses, increased as needed up to 2 mg/kg daily given in 2 divided doses. Maximum: 2 mg/kg daily. Course of therapy given for 15 to 20 wk with second course given, as needed, after a period of 2 mo or more off therapy.

Mechanism of Action

Inhibits sebaceous gland function and keratinization, which results in diminished nodular formation associated with recalcitrant nodular acne.

Contraindications

Hypersensitivity to isotretinoin or any of its components, hypersensitivity to parabens, pregnancy

Interactions

corticosteroids (systemic): Possibly increased risk of osteoporosis hormonal contraceptives including microdosed progesterone preparations, medroxyprogesterone injection, levonorgestrel implants: Possibly decreased effectiveness of contraceptive
phenytoin: Possibly increased risk of osteomalacia tetracyclines: Increased risk of benign intracranial hypertension vitamin A supplements: Increased risk of additive toxic effects

Side Efect

CNS: Aggressive or violent behavior, depression, dizziness, drowsiness, emotional instability, fatigue, headache, insomnia, lethargy, malaise, nervousness, paresthesias, pseudotumor cerebri, psychosis, seizures, stroke, suicidal ideation, syncope, weakness
CV: Chest pain, decreased high-density lipoprotein level, edema, elevated creatinine phosphokinase level, hypercholesteremia, hypertriglyceridemia, palpitation, stroke, tachycardia, vascular thrombotic disease, vasculitis
ENDO: Abnormal menses, alterations in blood glucose levels
EENT: Bleeding and inflammation of gums, cataracts, color vision disorder, conjunctivitis, corneal opacities, decreased night vision, dry mouth or nose, dry eyes, epistaxis, eyelid inflammation, hearing impairment, keratitis, optic neuritis, photophobia, tinnitus, visual disturbances, voice alteration
GI: Colitis, hepatitis, ileitis, inflammatory bowel disease, liver enzyme elevation, nausea, pancreatitis
GU: Glomerulonephritis, hematuria, proteinuria, WBCs in urine
HEME: Anemia, agranulocytosis, neutropenia, platelet count elevation, sedimentation rate elevation, thrombocytopenia
MS: Arthralgia, arthritis, back pain (children), bone abnormalities, calcification of tendons and ligaments, premature epiphyseal closure, tendonitis
RESP: Bronchospasms, respiratory infection
SKIN: Alopecia, bruising, disseminated herpes simplex, dry lips or skin, eczema, eruptive xanthomas, facial erythema, flushing, fulminant acne, hair abnormalities, hirsutism, hyperpigmentation, hypopigmentation, increased sunburn susceptibility, infections, nail dystrophy, paronychia, peeling of palms and soles, photoallergic or photosensitizing reactions, pruritus, pyogenic granuloma, rash, seborrhea, skin fragility, sweating, urticaria
Other: Abnormal wound healing, alkaline phosphatase increase, allergic reactions, hyperuricemia, lymphadenopathy, weight loss

Cautions

Ensure that women of childbearing age have had two negative urine or serum pregnancy tests with a sensitivity of at least 50 mIU/ml, joined the Accutane Survey, signed the consent form, and watched the videotape provided by manufacturer prior to beginning isotretinoin therapy. isotretinoin 551 G H I
WARNING Notify prescriber if elevated serum triglyceride levels can’t be controlled or if symptoms of pancreatitis occur (abdominal pain, nausea, vomiting). Drug may need to be discontinued because fatal hemorrhagic pancreatitis has occurred with drug use.

Obtain serum lipid level before therapy and periodically thereafter, as ordered, to detect elevated lipid levels that result from isotretinoin therapy.

Monitor liver enzyme levels periodically, as ordered, because drug can cause hepatitis.

Assess patient frequently for adverse reactions and report to prescriber any that occur; drug may have serious adverse effects that require discontinuation.

PATIENT SAFTY

Instruct patient to take isotretinoin with food or milk.

Advise women of childbearing age that two forms of contraceptives must be used simultaneously (unless absolute abstinence is the chosen method) 1 month before therapy and for 1 month after therapy has stopped because of potential for fetal harm. Inform women who use oral contraceptives that drug may lessen effectiveness of oral contraceptives. Urge patient to notify prescriber immediately if pregnancy occurs.

Stress importance of picking up isotretinoin prescription within 7 days of a pregnancy test or, for male patients or women not of childbearing potential, within 30 days of prescription.

Urge patient to report headache, nausea, vomiting and visual disturbances immediately to prescriber because drug will need to be discontinued immediately and patient referred to a neurologist.

Caution patient and family that isotretinoin may cause aggressive or violent behavior, depression, psychosis, and suicidal ideation. Instruct patient to notify prescriber immediately if changes in mood occur.

Tell patient to report hearing changes or tinnitus, visual difficulties, abdominal pain, rectal bleeding, or severe diarrhea to prescriber because drug may need to be discontinued.

Advise patient to avoid hazardous activities until drug’s CNS effects are known. Caution that changes in night vision may occur suddenly.

Caution patient not to donate blood during therapy and for 1 month after therapy has stopped because blood might be given to a pregnant woman.

Warn patient that transient exacerbation of acne may occur, especially during initial therapy and to notify prescriber if this occurs.

Instruct patient to avoid wax epilation and skin resurfacing procedures during therapy and for at least 6 months thereafter because of scarring potential.

Caution patient to avoid exposure to direct sunlight or UV light and to wear sunscreen when outdoors.

Inform patient that contact lens tolerance may decrease during and after isotretinoin therapy.

Alert patient to the potential for mild musculoskeletal

Side Efect

, which usually clear rapidly after drug is discontinued. Urge patient to notify prescriber if symptoms become bothersome or serious because drug may need to be discontinued.

Advise patient not to take vitamin A supplements while on isotretinoin therapy because of potentially additive toxic effects.

Instruct patient to notify all prescribers of isotretinoin use because of the risk of interactions.

Inform patient of need for frequent laboratory tests and importance of complying with scheduled appointments.

Category

Chemical class: Dihydropyridine derivative
Therapeutic class: Antihypertensive

Pregnancy category: C

Indications

To manage essential hypertension
Adults. Initial: 2.5 mg b.i.d., increased by 5 mg every 2 to 4 wk, if needed. Maximum: 20 mg daily. isradipine 552

Mechanism of Action

Inhibits calcium movement into coronary vascular smooth-muscle cells by blocking the slow calcium channels in their membranes. By decreasing intracellular calcium level, isradipine inhibits smooth-muscle cell contractions. The result is relaxation of coronary and vascular smooth muscle, decreased peripheral vascular resistance, and reduced systolic and diastolic blood pressure, all of which decrease myocardial oxygen demand. Route Onset Peak Duration P.O. 2–3 hr 2–4 wk Unknown

Contraindications

Hypersensitivity to isradipine or its components

Interactions

anesthetics (hydrocarbon inhalation), antihypertensives, hydrochlorothiazide, prazocin: Increased risk of hypotension
beta blockers: Increased adverse effects of beta blockers
cimetidine: Increased blood level and bioavailability of isradipine digoxin: Transiently increased blood digoxin level and risk of digitalis toxicity estrogens: Possibly increased fluid retention and decreased isradipine effects lithium: Increased risk of neurotoxicity NSAIDs, sympathomimetics: Possibly decreased therapeutic effects of isradipine procainamide,
quinidine: Increased risk of prolonged QT interval grapefruit juice: Doubled isradipine bioavailability other : Prolonged time to achieve peak blood level

Side Efect

CNS: Asthenia, dizziness, fatigue, headache, paresthesia, somnolence, stroke, syncope, transient ischemic attack, weakness
CV: Angina, atrial fibrillation, heart failure, hypotension, MI, orthostatic hypotension, palpitations, peripheral edema, tachycardia, ventricular fibrillation
EENT: Gingival hyperplasia, pharyngitis, rhinitis
GI: Abdominal cramps, constipation, diarrhea, elevated liver function test results, indigestion, nausea, vomiting
HEME: Leukopenia
MS: Back pain
RESP: Cough
SKIN: Flushing, photosensitivity, rash, urticaria
Other: Angioedema

Cautions

Monitor blood pressure and heart rate often during isradipine therapy.

Monitor patient with impaired hepatic or renal function for an increased blood isradipine level.

Avoid giving isradipine with food because doing so increases time to peak effect by about 1 hour.

Observe for mild peripheral edema caused by vasodilation of small blood vessels. Know that this type of edema doesn’t result from fluid retention or heart failure.

PATIENT SAFTY

Inform patient that isradipine therapy will be long-term and will require laboratory tests and follow-up visits to monitor drug effects.

Instruct patient to take drug exactly as prescribed and to swallow capsules whole, not crushing or chewing them.

Advise patient to take drug on an empty stomach 1 hour before or 2 hours after meals.

Instruct patient to take a missed dose as soon as he remembers it unless it’s nearly time for the next dose. In that case, advise him to wait and take next scheduled dose, but not to double the dose. If more than one dose is missed, tell him to contact prescriber.
WARNING Urge patient not to stop taking drug suddenly. Doing so may lead to lifethreatening problems.

Inform patient that fragments of capsules may be visible in stool.

Caution patient not to drink grapefruit juice during isradipine therapy.

Urge patient to avoid potentially hazardous activities until isradipine’s CNS effects are known.

Caution patient to change position slowly to minimize orthostatic hypotension.

Urge patient to contact prescriber if he isradipine 553 G H I experiences chest pain, fainting, irregular heartbeat, rash, or swollen ankles while taking isradipine.

Instruct patient to maintain good oral hygiene, perform gum massage, and see a dentist every 6 months to prevent gum bleeding and gum disorders.

To help prevent photosensitivity reactions, caution patient to avoid direct sunlight and to wear protective clothing and apply sunscreen when outdoors.

Instruct patient to store drug at room temperature in a dry place.

Category

Chemical class: Triazole derivative
Therapeutic class: Antifungal

Pregnancy category: C

Indications

To treat blastomycosis caused by Blastomyces dermatitidis and histoplasmosis caused by Histoplasma capsulatum Adults and adolescents. Initial: 200 mg daily, increased by 100 mg daily, if needed. Maximum: 400 mg daily, with dosage greater than 200 mg given in divided doses b.i.d. To treat aspergillosis unresponsive to amphotericin B Adults and adolescents.200 to 400 mg daily, with dosage greater than 200 mg daily given in divided doses b.i.d. To treat oropharyngeal candidiasis

ORALL

Adults and adolescents. 100 mg b.i.d. for 7 to 14 days. To treat esophageal candidiasis

ORALL

Adults and adolescents.100 mg daily for at least 3 wk and continued for 2 wk after symptoms resolve. To treat onychomycosis of toenails only or of toenails and fingernails Adults and adolescents.200 mg daily for 12 wk. To treat onychomycosis of fingernails only Adults and adolescents.200 mg b.i.d. for 7 days; then repeated after 3 wk.

Mechanism of Action

Inhibits the synthesis of ergosterol, an essential component of fungal cell membranes, by binding with a cytochrome P450 enzyme needed to convert lanosterol to ergosterol. Lack of ergosterol results in increased cellular permeability and leakage of cell contents. Itraconazole also may lead to fungal cell death by inhibiting fungal respiration under aerobic conditions.

Contraindications

Concurrent therapy with cisapride, dofetilide, ergot alkaloids, HMG-CoA inhibitors (lovastatin and simvastatin), levomethadyl, nisoldipine, oral midazolam, pimozide, quinidine, or triazolam; evidence of ventricular dysfunction, as in congestive heart failure (CHF) or a history of it (onychomycosis treatment); hypersensitivity to itraconazole or its components; planning for pregnancy during onychomycosis treatment

Interactions

alfentanil, buspirone, busulfan, carbamazepine, cyclosporine, digoxin, docetaxel, indinavir, methylprednisolone, phenytoin, pimozide, rifabutin, ritonavir, saquinavir, sirolimus, tacrolimus, trimetrexate, vinca alkaloids: Possibly increased blood levels of these and serious adverse effects alprazolam, diazepam, oral midazolam, triazolam: Elevated blood levels and possibly prolonged sedative effects of these antacids, anticholinergics, H2-receptor antagonists, omeprazole, sucralfate: Possibly decreased itraconazole absorption atorvastatin, lovastatin, simvastatin: Increased blood levels of these ; possibly rhabdomyolysis calcium channel blockers: Possibly edema and increased blood levels of these carbamazepine, isoniazid, nevirapine, phenobarbital, phenytoin, rifabutin,
rifampin: Possibly decreased blood itraconazole level cilostazol; eletriptan; glucocorticosteroids such as budesonide, dexamethasone, fluticasone, and methylprednisolone; trimetrexate: itraconazole 554 Possibly inhibited metabolism of these cisapride, dofetilide, disopyramide, halofantrine, levomethadyl, pimozide,
quinidine: Possibly increased plasma levels of these leading to potentially life-threatening cardiovascular complications such as cardiac arrest, prolonged QT interval, torsades de pointes, ventricular tachycardia, and sudden death clarithromycin, erythromycin, indinavir, ritonavir: Possibly increased blood itraconazole level didanosine: Possibly decreased therapeutic effects of itraconazole ergot alkaloids: Possibly increased plasma ergot alkaloid elevation leading to cerebral ischemia and ischemia of the extremities fentanyl: Possibly increased plasma fentanyl level causing potentially fatal respiratory depression nisoldipine: Increased plasma nisoldipine levels that do not decrease after drug dosage is reduced oral antidiabetic : Possibly increased blood levels of these and risk of hypoglycemia
warfarin: Increased anticoagulant effect of warfarin

Side Efect

CNS: Dizziness, drowsiness, fatigue, fever, headache, paresthesia, peripheral neuropathy, vertigo
CV: CHF, hypertriglyceridemia, hypertension, peripheral edema
EENT: Blurred vision, diplopia, transient or permanent hearing loss, tinnitis
GI: Abdominal pain, anorexia, constipation, diarrhea, elevated liver function test results, flatulence, hepatic failure, hepatitis, hepatotoxicity, hyperbilirubinemia, indigestion, nausea, vomiting
GU: Erectile dysfunction, menstrual irregularities, urinary incontinence
HEME: Leukopenia, neutropenia, thrombocytopenia
MS: Arthralgia, myalgia
RESP: Cough, dyspnea, pulmonary edema
SKIN: Alopecia, diaphoresis, erythema multiforme, exfoliative dermatitis, leukocytoclastic vasculitis, photosensitivity, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, hypokalemia, serum sickness

Cautions

Use itraconazole with extreme caution in patients with risk factors for CHF, such as ischemic or valvular heart disease, significant COPD, and renal failure and other edematous disorders because of increased risk of developing CHF during itraconazole treatment.

Use itraconazole cautiously in patients with hypersensitivity to other azole antifungals (because cross-hypersensitivity is unknown) and in patients with renal or hepatic impairment.

Because itraconazole has been linked to serious adverse cardiac and hepatic effects, expect to send appropriate nail specimens for laboratory testing to confirm onychomycosis before beginning therapy.
WARNING Keep in mind that itraconazole is a potent inhibitor of the cytochrome P-450 3A4 (CYP3A4) isoenzyme system,which may increase blood levels of metabolized by this system.Patients taking such as cisapride with itraconazole or other CYP3A4 inhibitors have experienced life-threatening cardiovascular complications,such as prolonged QT interval,torsades de pointes,and ventricular tachycardia,as well as sudden death.

Administer itraconazole capsules (not oral solution) with a meal to ensure maximal absorption.

Keep in mind that a patient with AIDS may have hypochlorhydria, which reduces drug absorption. For such a patient, expect to administer higher doses of itraconazole.

Monitor liver function test results in patients with impaired hepatic function and those who have experienced hepatotoxicity with other .

If patient develops signs and symptoms of peripheral neuropathy or CHF, such as fatigue, dyspnea, and peripheral edema, expect to discontinue drug.

Assess patient for rash every 8 hours during therapy; notify prescriber if rash occurs.

If patient also receives warfarin, monitor PT and assess patient for signs and symptoms of bleeding. itraconazole 555 G H I

If patient also receives digoxin, monitor blood digoxin level as appropriate to detect toxic level, and assess patient for signs and symptoms of digitalis toxicity, such as nausea and yellow vision.

PATIENT SAFTY

Instruct patient to take itraconazole capsules with a meal, but oral solution without food.

If patient also takes an oral antidiabetic drug, instruct him to check his blood glucose level often because of the increased risk of hypoglycemia.

Advise patient to avoid taking antacids with oral itraconazole.

Advise patient to notify prescriber immediately of changes in other , such as new and dosage changes.

Advise patient to notify prescriber immediately about abdominal pain, diarrhea, headache, hearing loss, nausea, peripheral neuropathy, rash, or vomiting.

Instruct patient to notify prescriber if he experiences signs of liver problems, such as abdominal pain, dark urine, fatigue, loss of appetite, pale stools, weakness, or yellow eyes or skin.

Caution breast-feeding patient to consult prescriber about continuation of breastfeeding during itraconazole therapy.

Category

Chemical class: Aminoglycoside
Therapeutic class: Antibiotic

Pregnancy category: D

Indications

To treat infections caused by gramnegative organisms (including Acinetobacter species, Enterobacter aerogenes, Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Neisseria species, Proteus species, Providencia species, Salmonella species, Serratia marcescens, Shigella species, and Yersinia species) and gram-positive organisms (including Staphylococcus aureus and Staphylococcus epidermidis)
I.M.INJECTION Adults and children. 3.75 mg/kg every 6 hr, 5 mg/kg every 8 hr, or 7.5 mg/kg every 12 hr for 7 to 10 days. Maximum: 1.5 g daily.
IV: Adults and children.5 mg/kg every 8 hr or 7.5 mg/kg every 12 hr for 7 to 10 days. Maximum: 1.5 g daily. As adjunct to suppress intestinal bacterial growth
Adults. 1 g/hr for 4 hr and then 1 g every 6 hr for 36 to 72 hr. To treat hepatic coma
Adults.8 to 12 g daily in divided doses. To treat respiratory tract infection INHALATION NEBULIZER
Adults.250 mg b.i.d. to q.i.d. Maximum: 1.5 g daily.
DOSAGE ADJUSTMENT For elderly patients and those with renal failure, dosage reduced and blood kanamycin level and renal function test results monitored.

Mechanism of Action

Binds to negatively charged sites on bacterial outer cell membranes, which disrupts cell membrane integrity. Kanamycin also binds to bacterial ribosomal subunits and inhibits protein synthesis; these actions lead to cell death. Route Onset Peak Duration P.O. Slow Unknown Unknown I.V. Rapid Unknown Unknown I.M. Unknown 1–2 hr Unknown

Incompatibilities

Don’t mix kanamycin in same syringe or administer through same I.V. line as other antibiotics.

Contraindications

Hypersensitivity to kanamycin, other aminoglycosides, or their components; intestinal obstruction (oral form)

Interactions

cephalosporins, vancomycin: Increased risk of nephrotoxicity digoxin, loop diuretics: Increased ototoxic and nephrotoxic effects of kanamycin general anesthetics, neuromuscular blockers: Increased risk of neuromuscular blockade penicillins: Inactivation of kanamycin or synergistic effects

Side Efect

CNS: Ataxia, dizziness, headache
EENT: Hearing loss
GI: Diarrhea
GU: Elevated BUN and serum creatinine levels, oliguria, proteinuria
MS: Muscle paralysis
RESP: Apnea
SKIN: Injection site irritation or pain

Cautions

Obtain body fluid or tissue specimen for culture and sensitivity testing before kanamycin therapy begins, as indicated. Therapy may begin before test results are available.

Administer I.M. injection deep into upper outer quadrant of gluteus maximus. Rotate injection sites.

Be aware that oral kanamycin is minimally absorbed from intact GI mucosa but may be more absorbed from mechanically irrigated areas of the GI tract.

For I.V. use, dilute 500-mg vial with 100 to 200 ml normal saline solution or D5W, or 1-g vial with 200 to 400 ml normal saline or D5W, and infuse over 30 to 60 min.Vial contents may darken during storage but potency isn’t affected.

Keep patient well hydrated before and during therapy.

Monitor blood kanamycin level periodically during therapy, as appropriate.

Prolonged treatment increases risk of ototoxicity and nephrotoxicity. Monitor hearing and renal function if therapy lasts longer than 10 days.

PATIENT SAFTY

Explain need to take kanamycin at prescribed intervals around the clock until patient completes full course of therapy.

Advise patient to report dizziness, hearing loss, and severe diarrhea or headache.

Category

Chemical class: Propionic acid derivative
Therapeutic class: Analgesic, antiinflammatory

Pregnancy category: B

Indications

To treat symptoms of rheumatoid arthritis ,
Adults. Initial: 75 mg t.i.d. or 50 mg q.i.d. Maximum: 300 mg daily.
Adults. Maintenance: 150 to 200 mg daily. Maximum: 300 mg daily. To relieve pain in dysmenorrhea
Adults. Initial: 25 to 50 mg every 6 to 8 hr p.r.n. Maximum: 300 mg daily.
DOSAGE ADJUSTMENT Dosage reduced by 33% to 50% for patients with renal impairment.

Mechanism of Action

Blocks activity of cyclooxygenase, the enzyme needed for prostaglandin synthesis. Prostaglandins, important mediators of inflammatory response, cause local vasodilation with swelling and pain. By blocking cyclooxygenase and inhibiting prostaglandins, this NSAID reduces inflammatory symptoms and relieves pain.

Contraindications

Angioedema; aspirin-, iodide-, or NSAIDinduced asthma, bronchospasm, nasal polyps, rhinitis, or urticaria; hypersensitivity to ketoprofen or its components

Interactions

ACE inhibitors: Possibly decreased hypotensive effect of ACE inhibitors acetaminophen: Possibly increased adverse renal effects with long-term acetaminophen use aspirin, other
NSAIDs: Increased risk of bleeding and adverse GI effects, increased and prolonged blood ketoprofen levels cefamandole, cefoperazone, cefotetan: Increased risk of hypoprothrombinemia and bleeding colchicine, platelet aggregation inhibitors: Increased risk of GI bleeding, hemorrhage, and ulcers corticosteroids, potassium supplements: Increased risk of adverse GI effects cyclosporine: Increased risk of nephrotoxicity from both , increased blood cyclosporine level diuretics (loop, potassium-sparing, and thiazide): Decreased diuretic and antihypertensive effects gold compounds, nephrotoxic : Increased risk of adverse renal effects heparin, oral anticoagulants, thrombolytics: Increased anticoagulant effects, increased risk of hemorrhage insulin, oral antidiabetic : Possibly increased hypoglycemic effects of these lithium: Increased blood lithium level and possibly toxicity methotrexate: Decreased methotrexate clearance, increased risk of methotrexate toxicity plicamycin,
valproic acid: Increased risk of hypoprothrombinemia and GI bleeding, hemorrhage, and ulcers probenecid: Possibly increased blood level, effectiveness, and risk of toxicity of ketoprofen
alcohol use: Increased risk of adverse GI effects ketoprofen 558

Side Efect

CNS: Headache, irritability, nervousness, seizures, stroke
CV: Edema, fluid retention, hypertension, MI, tachycardia
EENT: Tinnitus, vision changes
GI: Abdominal pain, anorexia, constipation, diarrhea, diverticulitis, dyspepsia, dysphagia, flatulence, gastritis, gastroenteritis, gastroesophageal reflux disease, GI bleeding and ulceration, hepatic failure, hiatal hernia, indigestion, melena, nausea, perforation of stomach or intestine, stomatitis, vomiting
GU: Acute renal failure, decreased urine output
HEME: Agranulocytosis, anemia, easy bruising, hemolytic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia
RESP: Asthma, respiratory depression
SKIN: Erythema multiforme, StevensJohnson syndrome, toxic epidermal necrolysis, rash
Other: Anaphylaxis, angioedema, rapid weight gain

Cautions

Use ketoprofen with extreme caution in patients with history of ulcer disease or GI bleeding because NSAIDs such as ketoprofen increase risk of GI bleeding and ulceration. Expect to use ketoprofen for shortest time possible in these patients.

Be aware that serious GI tract ulceration, bleeding, and perforation may occur without
WARNING symptoms. Elderly patients are at greater risk. To minimize risk, give drug with food. If GI distress occurs, withhold drug and notify prescriber immediately.

Use ketoprofen cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.
WARNING Monitor patient closely for thrombotic events, including MI and stroke, because NSAIDs increase the risk.

Monitor patient—especially if he’s elderly or receiving long-term ketoprofen therapy—for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results because, rarely, elevations may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in elderly patients, patients taking diuretics or ACE inhibitors, and patients with heart failure, impaired renal function, or hepatic dysfunction; drug may cause renal failure.

Monitor CBC for decreased hemoglobin level and hematocrit because drug may worsen anemia.
WARNING If patient has bone marrow suppression or is receiving an antineoplastic drug, monitor laboratory results (including WBC count), and watch for evidence of infection because anti-inflammatory and antipyretic actions of ketoprofen may mask signs and symptoms, such as fever and pain.

Assess patient’s skin regularly for signs of rash or other hypersensitivity reaction because ketoprofen is an NSAID and may cause serious skin reactions without warning, even in patients with no history of NSAID sensivitity. At first sign of reaction, stop drug and notify prescriber.

If patient takes acetaminophen, monitor fluid intake and output, BUN level, and serum creatinine level for evidence of adverse renal effects.

PATIENT SAFTY

Instruct patient to take ketoprofen with food or after meals to prevent GI upset. Advise him to take drug with a full glass of water and to avoid lying down for 15 to 30 minutes afterward to prevent drug from lodging in esophagus and causing irritation.

Advise patient to swallow drug whole and not to crush, break, chew, or open capsules.

Instruct patient to avoid aspirin, aspirincontaining products, and alcohol while taking ketoprofen to decrease risk of adverse GI effects.

Tell patient not to take more drug than prescribed because stomach bleeding may occur.

If patient takes an anticoagulant, tell him to watch for and immediately report bleeding problems, such as bloody or tarry stools and bloody vomitus.

If patient takes insulin or an oral antidiabetic, advise him to monitor blood glucose level closely. Urge him to carry candy or other simple sugars to treat mild hypoglycemia. If he has frequent or severe episodes, instruct him to consult prescriber.

Inform patient that he may be nervous and irritable while taking ketoprofen.

Instruct patient to notify prescriber immediately if he develops a rash, decreased urine output, dark yellow or brown urine, or signs of fluid retention, including swelling of extremities and unexplained rapid weight gain.

Caution pregnant patient not to take NSAIDs such as ketoprofen during last trimester because they may cause premature closure of the ductus arteriosus.

Explain that ketoprofen may increase risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.

Explain that ketoprofen may increase risk of serious adverse GI reactions; stress importance of seeking immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.

Alert patient to rare but serious skin reactions. Urge him to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity.

Category

Chemical class: Acetic acid derivative
Therapeutic class: Analgesic, antiinflammatory

Pregnancy category: C

Indications

To treat moderate to severe pain Adults ages 16 to 64. Initial: 20 mg as single dose, followed by 10 mg every 4 to 6 hr p.r.n., up to 4 times a day. Maximum: 40 mg daily for no more than 5 days.
DOSAGE ADJUSTMENT For patients weighing less than 50 kg, elderly patients, and patients with impaired renal function, initial dose reduced to 10 mg.
I.M.INJECTION Adults ages 16 to 64. Initial: 60 mg as single dose, followed by oral ketorolac if needed; or 30 mg every 6 hr p.r.n. Maximum: 120 mg daily for no more than 5 days.
DOSAGE ADJUSTMENT For patients weighing less than 50 kg, elderly patients, and patients with impaired renal function, initial dose reduced to 30 mg, followed by oral ketorolac if needed; or 15 mg every 6 hr p.r.n., up to maximum of 60 mg daily for no more than 5 days.
I.V.INJECTION Adults ages 16 to 64. Initial: 30 mg as single dose, followed by oral ketorolac if needed; or 30 mg every 6 hr p.r.n. Maximum: 120 mg daily for no more than 5 days.
DOSAGE ADJUSTMENT For patients weighing less than 50 kg, elderly patients, and patients with impaired renal function, initial dose reduced to 15 mg, followed by oral ketorolac if needed; or 15 mg every 6 hr p.r.n., up to maximum of 60 mg daily for no more than 5 days. Route Onset Peak Duration P.O. 30–60 min 2–3 hr 5–6 hr I.M., I.V. 30–60 min 1–2 hr 4–6 hr

Mechanism of Action

Blocks cyclooxygenase, an enzyme needed to synthesize prostaglandins. Prostaglandins mediate inflammatory response and cause local vasodilation, swelling, and pain. They also promote pain transmission from periphery to spinal cord. By blocking cyclooxygenase and inhibiting prostaglandins, this NSAID reduces inflammation and relieves pain.

Contraindications

Advanced renal impairment or risk of renal impairment due to volume depletion; before or during surgery if hemostasis is critical; breast-feeding; cerebrovascular bleeding; concurrent use of aspirin or other salicylates, other NSAIDs, or probenecid; ketorolac tromethamine 560 hemorrhagic diathesis; history of GI bleeding, GI perforation, or peptic ulcer disease; hemophilia or other bleeding problems, including coagulation or platelet function disorders; hypersensitivity to ketorolac tromethamine, aspirin, other NSAIDs, or their components; incomplete hemostasis; labor and delivery; treatment of perioperative pain during coronary artery bypass graft surgery

Interactions

ACE inhibitors, angiotensin II receptor antagonists: Increased risk of renal impairment; decreased effectiveness of these acetaminophen, gold compounds: Increased risk of adverse renal effects amphotericin, penicillamine, and other nephrotoxic : Increased risk or severity of adverse renal reactions antihypertensives, diuretics: Possibly reduced effects of these aspirin and other salicylates, other
NSAIDs: Additive toxicity cefamandole, cefoperazone, cefotetan: Possibly hypoprothrombinemia corticosteroids, potassium supplements: Increased risk of gastric ulcers or hemorrhage furosemide: Decreased effects of furosemide heparin, oral anticoagulants, platelet aggregation inhibitors, thrombolytics: Increased risk of GI bleeding and I.M. hematoma formation lithium: Possibly increased blood lithium level and increased risk of lithium toxicity methotrexate: Possibly methotrexate toxicity nondepolarizing muscle relaxants: Increased risk of apnea pentoxifylline, selective serotonin reuptake inhibitors: Increased risk of bleeding plicamycin,
valproic acid: Possibly hypoprothrombinemia and increased risk of bleeding probenecid: Decreased elimination of ketorolac, increased risk of adverse effects
alcohol use: Increased risk of adverse GI effects

Side Efect

CNS: Aseptic meningitis, cerebral hemorrhage, coma, dizziness, drowsiness, headache, psychosis, seizures, stroke
CV: Edema, fluid retention, hypertension
EENT: Laryngeal edema, stomatitis
ENDO: Hyperglycemia
GI: Abdominal pain; acute pancreatitis; bloating; constipation; diarrhea; diverticulitis; flatulence; GI bleeding, perforation, or ulceration; hepatitis; hepatic failure; jaundice; indigestion; nausea; perforation of stomach or intestines; vomiting; worsening of inflammatory bowel disease
GU: Interstitial nephritis, renal failure, urine retention
HEME: Agranulocytosis, anemia, aplastic or hemolytic anemia, eosinophilia, leukopenia, lymphadenopathy, pancytopenia, thrombocytopenia
RESP: Bronchospasm, pneumonia, respiratory depression
SKIN: Diaphoresis, erythema multiforme, exfoliative dermatitis, photosensitivity, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, hyperkalemia, hyponatremia, injection site pain, sepsis, unusual weight gain

Cautions

Read ketorolac label carefully. Don’t use I.M. form for I.V. route. Know that ketorolac isn’t for intrathecal or epidural use.

Inject I.M. ketorolac slowly, deep into a large muscle mass. Monitor site for bleeding, bruising, or hematoma.

Give I.V. injection over at least 15 seconds.

Notify prescriber if pain relief is inadequate or if breakthrough pain occurs between doses because supplemental doses of an opioid analgesic may be required.
WARNING Monitor liver function test results. If elevated levels persist or worsen, notify prescriber and expect to stop drug, as ordered, to prevent hepatic impairment.
WARNING Monitor patients with a history of peripheral edema, heart failure, or hypertension for adequate fluid balance because drug can promote fluid retention and worsen these conditions. Assess patient for dyspnea, edema, unexplained rapid weight gain, and decreased activity tolerance. Notify prescriber if such symptoms develop.

Use ketorolac with extreme caution in patients with history of ulcer disease or GI bleeding because NSAIDs like ketorolac increase risk of GI bleeding and ulceration. Use ketorolac in these patients for shortest length of time possible.

Serious GI tract ulceration and bleeding and perforation of stomach or intestine can occur without
WARNING or symptoms. Elderly patients are at greater risk. To minimize risk, give drug with food. If GI distress occurs, withhold drug and notify prescriber immediately.

Monitor patient with history of inflammatory bowel disease, such as ulcerative colitis or Crohn’s disease, because ketorolac may worsen these conditions.

Use ketorolac cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy because drug can lead to onset of hypertension or worsen existing hypertension.
WARNING Monitor patient closely for thrombotic events including MI and stroke because NSAIDs such as ketorolac increase risk.

Monitor patient—especially if elderly—for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results because rarely, elevations may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in patients with heart failure, impaired renal function, or hepatic dysfunction; those who are taking diuretics or ACE inhibitors; and the elderly because drug may cause renal failure.

Monitor CBC for decreased hemoglobin and hematocrit because drug may worsen anemia.
WARNING In patient who has bone marrow suppression or is receiving antineoplastic drug therapy, monitor laboratory results (including WBC) and assess for evidence of infection because ketorolac has antiinflammatory and antipyretic actions that may mask signs and symptoms, such as fever and pain.

Assess patient’s skin routinely for rash or other evidence of hypersensitivity reactions because ketorolac is an NSAID and may cause serious skin reactions without
WARNING, even in patients with no history of NSAID hypersensitivity. Stop drug at first sign of reaction, and notify prescriber.

PATIENT SAFTY

Instruct patient to take ketorolac tablets with a meal, a snack, or an antacid to prevent stomach upset. Advise him to take drug with a full glass of water and to stay upright for at least 15 minutes afterward.

Advise patient not to take aspirin, other salicylates, or other NSAIDs while taking ketorolac without consulting prescriber. Urge patient to limit use of acetaminophen to only a few days during ketorolac therapy and to notify prescriber of use.

Instruct him to immediately report blood in urine, easy bruising, itching, rash, swelling, or yellow eyes or skin.

Caution pregnant patient that NSAIDs like ketorolac shouldn’t be taken during last trimester because drug may cause premature closure of the ductus arteriosus.

Explain that ketorolac may increase risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.

Tell patient that ketorolac also may increase risk of serious adverse GI reactions; stress importance of seeking immediate medical attention if signs or symptoms occur, such as epigastric or abdominal pain, indigestion, black tarry stools, and vomiting blood or coffee ground material.

Alert patient to the possibility of serious skin reactions, although rare, occurring with ketorolac therapy. Urge patient to seek immediate medical attention if signs or symptoms occur, such as a rash, blisters, fever, or other signs of hypersensitivity, such as itching.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Urge patient to avoid alcohol while taking ketorolac.

Encourage patient to have dental procedures performed before starting drug therapy because of increased risk of bleeding.

Teach patient proper oral hygiene measures, and encourage him to use a soft-bristled toothbrush while taking ketorolac.

Category

Chemical class: Benzamine derivative
Therapeutic class: Antihypertensive

Pregnancy category: C

Indications

To manage hypertension
Adults. Initial: 100 mg b.i.d., increased by 100 mg b.i.d. as needed and tolerated every 2 to 3 days. Maintenance: 200 to 400 mg b.i.d. For severe hypertension, 1.2 to 2.4 g daily in divided doses b.i.d. or t.i.d. To manage severe hypertension and treat hypertensive emergencies
IV:
Adults. 200 mg diluted in 160 ml of D5W and infused at 2 mg/min until desired response occurs.
I.V.INJECTION
Adults.20 mg given over 2 min; additional doses given in increments of 40 to 80 mg every 10 min as indicated until desired response occurs. Maximum: 300 mg. Route Onset Peak Duration P.O. 20 min– 1–4 hr 8–24 hr 2 hr I.V. 2–5 min 5–15 min 2–4 hr

Mechanism of Action

Selectively blocks alpha1and beta2receptors in vascular smooth muscle and beta1 receptors in heart to reduce peripheral vascular resistance and blood pressure. Potent beta blockade prevents reflex tachycardia, which commonly occurs when alpha blockers reduce resting heart rate, cardiac output, or stroke volume.

Incompatibilities

Don’t dilute labetalol in sodium bicarbonate solution or give through same I.V. line as alkaline , such as furosemide; doing so may cause white precipitate to form.

Contraindications

Asthma, cardiogenic shock, heart failure, hypersensitivity to labetalol or its components, secondor third-degree heart block, severe bradycardia

Interactions

allergen immunotherapy, allergenic extracts for skin testing: Increased risk of serious systemic reaction or anaphylaxis beta blockers, digoxin: Increased risk of bradycardia calcium channel blockers, clonidine, diazoxide, guanabenz, reserpine: Possibly hypotension
cimetidine: Possibly increased labetalol effects estrogens,
NSAIDs: Possibly reduced antihypertensive effect of labetalol general anesthetics: Increased risk of hypotension and myocardial depression insulin, oral antidiabetic : Increased risk of hyperglycemia nitroglycerin: Possibly hypertension phenoxybenzamine, phentolamine: Possibly additive alpha1-blocking effects sympathomimetics with alphaand betaadrenergic effects (such as pseudoephedrine): Possibly hypertension, excessive bradycardia, or heart block xanthines (aminophylline and theophylline): Possibly decreased therapeutic effects of both all food: Increased blood labetalol level
alcohol use: Increased labetalol effects

Side Efect

CNS: Anxiety, confusion, depression, dizziness, drowsiness, fatigue, paresthesia, syncope, vertigo, weakness, yawning
CV: Bradycardia, chest pain, edema, heart block, heart failure, hypotension, orthostatic hypotension, ventricular arrhythmias
EENT: Nasal congestion, taste perversion
GI: Elevated liver function test results, hepatic necrosis, hepatitis, indigestion, nausea, vomiting
GU: Ejaculation failure, impotence
RESP: Dyspnea, wheezing
SKIN: Jaundice, pruritus, rash, scalp tingling

Cautions

During I.V. labetalol use, monitor blood pressure according to facility policy, usually every 5 minutes for 30 minutes, then every 30 minutes for 2 hours, and then every hour for 6 hours.

Keep patient in supine position for 3 hours after I.V. administration.
WARNING Be aware that labetalol masks common signs of shock.

Monitor blood glucose level in diabetic patient because labetalol may conceal symptoms of hypoglycemia.

Be aware that stopping labetalol tablets abruptly after long-term therapy could result in angina, MI, or ventricular arrhythmias. Expect to taper dosage over 2 weeks while monitoring response.

PATIENT SAFTY

Advise patient to report confusion, difficulty breathing, rash, slow pulse, and swelling in arms or legs.

Caution patient not to stop drug abruptly because doing so could cause angina and rebound hypertension.

Suggest that patient minimize effects of orthostatic hypotension by rising slowly, avoiding sudden position changes, and taking labetalol at bedtime, if approved by prescriber.

Instruct diabetic patient to check blood glucose level often and to be alert for signs and symptoms of hypoglycemia.

Inform patient that scalp tingling may occur early in treatment but is transient.

Urge patient to avoid alcohol during labetalol therapy.

Category

Chemical class: Functionalized amino acid
Therapeutic class: Anticonvulsant

Pregnancy category: C

Indications

As adjunct to treat partial-onset seizures in patients with epilepsy Adults and adolescents age 17 and over. Initial: 50 mg b.i.d., increased by 100 mg/ day at weekly intervals based on response and tolerance. Maintenance: 200 to 400 mg daily.
IV: Adults and adolescents age 17 and over. Initial: 50 mg infused over 30 to 60 min b.i.d., increased by 100 mg/day at weekly intervals. Maintenance: 200 to 400 mg daily.
DOSAGE ADJUSTMENT For patients with creatinine clearance of 30 ml/min/1.73 m2or less, maximum is 300 mg daily.

Mechanism of Action

May selectively inactivate voltage-gated sodium channels, which prevents seizure activity by stabilizing hyperexcitable neuronal membranes and inhibiting repetitive neuronal firing in the brain.

Contraindications

Hypersensitivity to lacosamide and its components

Interactions

that may prolong the QT interval: Possibly further QT-interval prolongation

Side Efect

CNS: Asthenia, ataxia, attention deficit, cerebellar syndrome, confusion, depression, dizziness, feeling drunk, fever, headache, hypoaesthesia, impaired balance, irritability, memory impairment, mood alteration, paresthesia, somnolence, suicidal ideation, tremor, vertigo
CV: Palpitations, prolonged QT interval
EENT: Blurred vision, diplopia, dry mouth, nystagmus, oral hypoaesthesia, tinnitus
GI: Constipation, diarrhea, dyspepsia, nausea, vomiting
HEME: Anemia, neutropenia
MS: Dysarthria, muscle spasms
SKIN: Pruritus, rash
Other: Delayed multi-organ hypersensitivity reaction; injection site pain, irritation, and erythema

Cautions

Use cautiously in patients with conduction problems (such as AV block, sick sinus syndrome) and no pacemaker in place or in patients with severe cardiac disease (such as myocardial ischemia, heart failure). Lacosamide may affect conduction.

Use cautiously in patients with diabetic neuropathy or cardiovascular disease because drug may predispose them to atrial fibrillation or flutter. lacosamide 564

Watch patient closely for suicidal tendencies, particularly when therapy starts and dosage changes, because depression may worsen temporarily during these times and lead to suicidal ideation.

Be aware that lacosamide therapy should be discontinued gradually over at least 1 week to minimize seizure frequency.

Monitor patient closely for hypersensitivity reactions to lacosamide, such as rash, pruritus, and more than one organ abnormality, such as elevated liver enzymes and myocarditis or pancreatitis.

PATIENT SAFTY

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Encourage patient to carry medical identification that indicates her diagnosis and drug therapy.

Category

Chemical: Synthetic disaccharide sugar Therapeutic: Ammonia reducer, laxative

Pregnancy category: B

Indications

To treat constipation POWDER, SYRUP
Adults.Initial: 10 to 20 g daily, increased p.r.n. Maximum: 40 g daily. To prevent and treat hepatic encephalopathy POWDER, SYRUP
Adults. Initial: 20 to 30 g t.i.d. or q.i.d. until two or three soft stools occur daily. Usual: 60 to 100 g daily in divided doses. For acute episodes, 20 to 30 g every 2 hr initially to achieve rapid laxative effect and then reduced to usual dosage. RETENTION ENEMA
Adults. 200 g (300 ml) diluted in 700 ml water or normal saline solution and given every 4 to 6 hr, as needed.

Mechanism of Action

Arrives unchanged in the colon, where it breaks down into lactic acid and small amounts of formic and acetic acids, acidifying fecal contents. Acidification leads to increased osmotic pressure in the colon, which, in turn, increases stool water content and softens stool. Also, lactulose makes intestinal contents more acidic than blood. This prevents ammonia diffusion from intestine into blood, as occurs in hepatic encephalopathy. The trapped ammonia is converted into ammonia ions and, by lactulose’s cathartic effect, is expelled in feces with other nitrogenous wastes. Route Onset Peak Duration P.O. 24–48 hr Unknown Unknown

Contraindications

Hypersensitivity to lactulose or its components, low-galactose diet

Interactions

antacids, antibiotics (especially oral neomycin), other laxatives: Decreased effectiveness of lactulose

Side Efect

GI: Abdominal cramps and distention, diarrhea, flatulence
ENDO: Hyperglycemia
Other: Hypernatremia, hypokalemia, hypovolemia

Cautions

When giving lactulose by retention enema, use a rectal tube with a balloon to help patient retain enema for 30 to 60 minutes. If not retained for at least 30 minutes, repeat dose. Be sure to deflate balloon and remove rectal tube after completing administration.

Expect to periodically check serum electrolyte levels of elderly or debilitated patient who uses oral drug longer than 6 months.

Monitor blood ammonia level in patient with hepatic encephalopathy. Also watch for dehydration, hypernatremia, and hypokalemia when giving higher lactulose doses to treat this condition.

Monitor diabetic patient for hyperglycemia because lactulose contains galactose and lactose.

Plan to replace fluids if frequent bowel movements cause hypovolemia.

PATIENT SAFTY

Advise patient to take lactulose with food or dilute with juice to reduce sweet taste.

Direct patient not to use other laxatives while taking lactulose.

Instruct patient to report abdominal distention or severe diarrhea.

Advise diabetic patient to check blood glucose level often and to report hyperglycemia.

Instruct patient to increase fluid intake if frequent bowel movements occur.

Teach patient with chronic constipation the importance of exercising, increasing fiber in diet, and increasing fluid intake.

Inform patient that because oral lactulose must reach the colon to work, bowel movement may not occur for 24 to 48 hours after taking drug.

Category

Chemical class: Phenyltriazine
Therapeutic class: Anticonvulsant

Pregnancy category: C

Indications

As adjunct to treat partial seizures; to treat generalized seizures of LennoxGastaut syndrome; to treat primary generalized tonic-clonic seizures CHEWABLE , Adults and children age 12 and over taking valproate. 25 mg every other day for 2 wk, followed by 25 mg once daily for 2 wk. Increased by 25 to 50 mg every 1 to 2 wk, if needed. Maintenance: 100 to 400 mg daily. Children ages 2 to 12 taking valproate. 0.15 mg/kg daily as a single dose or in divided doses b.i.d. for 2 wk and then 0.3 mg/kg daily as single dose or in divided doses b.i.d. for next 2 wk. Increased by 0.3 mg/kg every 1 to 2 wk, if needed, to reach maintenance dosage. Maintenance: 1 to 5 mg/kg daily as single dose or in divided doses b.i.d. Maximum: 200 mg daily. Adults and children age 12 and over taking an antiepileptic drug other than carbamazepine,phenytoin,phenobarbital, primidone,or valproate. 25 mg once daily for 2 wk, followed by 50 mg once daily for 2 wk. Increased by 50 mg every 1 to 2 wk, if needed. Maintenance: 225 to 375 mg daily in 2 divided doses b.i.d. Maximum: 400 mg daily. Children ages 2 to 12 taking an an antiepileptic drug other than carbamazepine, phenytoin,phenobarbital,primidone,or valproate. 0.3 mg/kg daily in 1 or 2 divided doses for 2 wk; followed by 0.6 mg/kg daily in 2 divided doses for 2 wk. Increased by 0.6 mg/kg daily every 1 to 2 wk, if needed. Maintenance: 4.5 to 7.5 mg/kg daily in 2 divided doses. Maximum: 300 mg daily Adults and children age 12 and over taking carbamazepine,phenytoin,phenobarbital, or primidone but not valproate. 50 mg once daily for 2 wk and then 100 mg daily in divided doses b.i.d. for 2 wk. Increased by 100 mg every 1 to 2 wk, if needed. Maintenance: 300 to 500 mg daily in divided doses b.i.d. Maximum: 700 mg daily in divided doses b.i.d. Children ages 2 to 12 taking carbamazepine,phenytoin,phenobarbital,or primidone but not valproate. 0.6 mg/kg daily in divided doses b.i.d. for 2 wk and then 1.2 mg/kg daily in divided doses b.i.d. for 2 wk. Increased by 1.2 mg/kg every 1 to 2 wk, if needed to reach maintenance dosage. Maintenance: 5 to 15 mg/kg daily in divided doses b.i.d. Maximum: 400 mg daily. To treat partial seizures after conversion from carbamazepine, phenytoin, phenobarbital, primidone, or valproate CHEWABLE , Adults and adolescents age 16 and over converting from carbamazepine,phenytoin,phenobarbital,or primidone. 50 mg once daily for 2 wk, followed by 100 mg once daily for next 2 wk. Increased by 100 mg daily every 1 to 2 wk (while continuing to take carbamazepine, phenytoin, phenobarbital, or primidone), until usual maintenance dosage—500 mg daily in divided doses b.i.d.—is achieved. Then carbamazepine, phenytoin, phenobarbital, or primidone dosage tapered in 20% decrements weekly over 4 wk and then discontinued. Adults and adolescents age 16 and over converting from valproate. 25 mg every other day for 2 wk followed by 25 mg once daily for 2 wk. Then increased by 25 to 50 mg daily every 1 to 2 wk until dosage of 200 mg daily is achieved. At this time valproate dosage decreased to 500 mg daily by decrements no greater than 500 mg daily every wk and then maintained at 500 mg daily for 1 wk. After completion of week, lamotrigine dosage increased to 300 mg daily and maintained for 1 wk while valproate dosage decreased to 250 mg daily and maintained for 1 wk. Then lamotrigine dosage increased by 100 mg daily every wk to achieve maintenance dose of 500 mg daily. Once achieved, valproate therapy is discontinued. As maintenance therapy for bipolar 1 disorder to delay occurrence of mood episodes (depression, mania, hypomania, mixed episodes) CHEWABLE , Adults not taking carbamazepine,phenytoin,phenobarbital,primidone,rifampin, or valproate. 25 mg once daily for 2 wk, followed by 50 mg once daily for 2 wk, followed by 100 mg once daily for 1 wk and then increased to 200 mg once daily as maintenance dose. Maximum: 200 mg daily. Adults taking valproate.25 mg every other day for 2 wk, followed by 25 mg once daily for 2 wk, followed by 50 mg once daily for 1 wk, and then increased to 100 mg once daily as maintenance dose. Adults taking carbamazepine,phenytoin, phenobarbital,primidone,or rifampin, but not valproate.50 mg once daily for 2 wk followed by 100 mg once daily in divided doses for 2 wk, followed by 200 mg once daily in divided doses for 1 wk and then increased to 300 mg daily in divided doses for 1 wk and then increased to 400 mg daily in divided doses as maintenance dose.
DOSAGE ADJUSTMENT For patient starting or stopping estrogen-containing oral contraceptives, lamotrigine dosage may need to be adjusted on individual basis. For patient with moderate to severe liver impairment without ascites, dosage reduced by 25%. For patient with severe liver impairment with ascites, dosage reduced by 50%.

Mechanism of Action

May stabilize neuron membranes by blocking their sodium channels and inhibiting release of excitatory neurotransmitters, such as glutamate and aspartate, through these channels. By blocking the release of neurotransmitters, lamotrigine inhibits the spread of seizure activity in the brain and reduces seizure frequency. Route Onset Peak Duration P.O. Days to Unknown Unknown wks

Contraindications

Hypersensitivity to lamotrigine or its components

Interactions

acetaminophen (long-term use): Possibly decreased blood lamotrigine level carbamazepine: Decreased blood lamotrigine level; possibly increased risk of dizziness, diplopia, ataxia, and blurred vision folate inhibitors, such as co-trimoxazole and methotrexate: Increased blood lamotrigine level oral contraceptives: Decreased blood lamotrigine level during 3 weeks of active hormonal therapy and increased blood lamotrigine level during 1 week of inactive hormonal therapy; possibly reduced effectiveness of oral contraceptives oxcarbazepine: Possibly increased risk of headache, dizziness, nausea, and somnolence phenobarbital, phenytoin, primidone: Decreased blood lamotrigine level, possibly increased CNS depression topiramate: Increased topiramate level
valproic acid: Increased lamotrigine level, decreased lamotrigine clearance, decreased blood valproic acid level
alcohol use: Possibly increased CNS depression

Side Efect

CNS: Amnesia, anxiety, ataxia, confusion, depression, dizziness, drowsiness, emotional lability, fever, headache, increased seizure activity, lack of coordination, suicidal ideation
CV: Chest pain
EENT: Blurred vision, diplopia, dry mouth, nystagmus
GI: Abdominal pain, anorexia, constipation, diarrhea, hepatic failure, vomiting
HEME: Anemia, aplastic anemia, disseminated intravascular coagulation, eosinophilia, leukopenia, neutropenia, pancytopenia, pure red cell aplasia, thrombocytopenia
SKIN: Petechiae, photosensitivity, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Acute multiorgan failure, angioedema, flulike symptoms, lymphadenopathy

Cautions

Use cautiously in patients with illnesses that could affect metabolism or elimination of lamotrigine, such as renal, hepatic, or cardiac functional impairment.
WARNING Lamotrigine may cause potentially life-threatening rash. Notify prescriber at first sign, and expect to discontinue drug. Lamotrigine therapy shouldn’t be restarted after rash subsides.

Monitor patient for

Side Efect

, especially suicidal thoughts, at start of therapy and with each dosage increase.

Monitor patient for seizure activity during lamotrigine therapy.

Stopping lamotrigine abruptly may increase seizure activity. Expect to taper dosage over at least 2 weeks, even for treatment of bipolar disorder.

PATIENT SAFTY

Advise patient to take lamotrigine exactly as prescribed and not to stop abruptly because seizure activity may increase.

Advise patient to notify prescriber immediately if rash occurs.

Instruct patient to report increased seizure activity, vision changes, and vomiting.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to avoid direct sunlight and to wear protective clothing to minimize risk of photosensitivity.

Instruct patient to wear or carry medical identification stating that she takes an anticonvulsant.

Caution patient or caregiver about possibility of suicidal thoughts, especially when therapy begins or dosage changes.

Tell female patient to notify prescriber if she becomes pregnant, is considering pregnancy, or starts or stops an oral hormonal contraceptive or other female hormonal preparation.

Urge woman who becomes pregnant while taking lamotrigine to enroll in the North American antiepileptic drug pregnancy registry by calling 1-888-233-2334. Explain that registry is collecting information about safety of antiepileptic during pregnancy.

Category

Chemical class: Somatostatin analog
Therapeutic class: Growth inhibitor

Pregnancy category: C

Indications

To treat acromegaly in patients with an inadequate response to or who cannot be treated with surgery or radiation SUBCUTANEOUS INJECTION
Adults.Initial: 90 mg every 4 wk for 3 mo; then dosage adjusted according to growth hormone (GH) level. If GH level is less than 1 nanogram/ml, dosage reduced to 60 mg every 4 wk. If GH level is 1 to 2.5 nanograms/ml, dosage is 90 mg every 4 wk. If GH level is above 2.5 nanograms/ml, dosage increased to 120 mg every 4 wk.
DOSAGE ADJUSTMENT For patient with moderate to severe renal or hepatic failure, initial dose reduced to 60 mg every 4 wk for 3 mo; then adjusted according to GH level.

Mechanism of Action

Reduces growth hormone (GH) and insulin growth factor-1 levels, allowing for normalization of these hormones in patients with acromegaly. An octapeptide analog of natural somatostatin, lanreotide has a high affinity for human somatostatin receptors 2 and 5. Activity at these receptors may be responsible for GH inhibition.

Contraindications

Hypersensitivity to lanreotide or its components

Interactions

beta blockers, calcium channel blockers:Additive depressive effects on heart rate bromocriptine: Possibly increased action of bromocriptine cyclosporine: Possibly decreased cyclosporine effectiveness metabolized by the liver, quinidine, terfenadine: Possibly increased blood levels of these insulin, oral antidiabetic : Possibly decreased effectiveness of these oral : Possibly decreased absorption of these

Side Efect

CNS: Headache
CV: Bradycardia, hypertension
ENDO: Hyperglycemia, hypoglycemia
GI: Abdominal pain, cholelithiasis, constipation, diarrhea, flatulence, loose stools, nausea, vomiting
HEME: Anemia
MS: Arthralgia
SKIN: Erythema, pruritus
Other: Injection site reactions (induration, pain, pruritus, redness, swelling), weight loss

Cautions

Check patient’s blood glucose level before starting lanreotide therapy and whenever dosage changes because drug may cause hypoglycemia or hyperglycemia.

Inject drug deep into subcutaneous tissue of upper, outer quadrant of buttock. Do not fold the skin. Insert needle perpendicular to the skin, rapidly and to its full length. Alternate between left and right buttocks.

If patient has underlying cardiovascular disease, watch for changes in heart rate and blood pressure because drug may cause bradycardia or hypertension.

Monitor patient’s GH and insulin growth factor-1 levels, as ordered, to assess lanreotide’s effects.

PATIENT SAFTY

Inform patient that lanreotide will be given as a subcutaneous injection every 4 weeks and that it may cause discomfort at the site.

Tell patient that periodic blood tests will be needed to monitor lanreotide’s effectiveness.

Instruct diabetic patient to monitor blood glucose level closely.

Category

Chemical class: Substituted benzimidazole
Therapeutic class: Antisecretory, antiulcer

Pregnancy category: B

Indications

To treat duodenal ulcers and maintain healed duodenal ulcers DELAYED-RELEASE , DELAYED-RELEASE SUSPENSION, DELAYED-RELEASE ORALLY

Adults.15 to 30 mg daily before morning meal for 4 wk. Maximum: 30 mg daily. To treat gastric ulcers DELAYED-RELEASE , DELAYED-RELEASE SUSPENSION, DELAYED-RELEASE ORALLY

Adults.15 to 30 mg daily before morning meal for up to 8 wk. To treat gastroesophageal reflux disease DELAYED-RELEASE , DELAYED-RELEASE SUSPENSION, DELAYED-RELEASE ORALLY

Adults.15 mg daily before morning meal for up to 8 wk. To treat non-erosive gastroesophageal reflux disease (DEXLANSOPRAZOLE)
Adults. 30 mg once daily for 4 wk. To heal all grades of erosive esophagitis (DEXLANSOPRAZOLE)
Adults.60 mg once daily for up to 8 wk. To maintain healed erosive esophagitis (DEXLANSOPRAZOLE)
Adults. 30 mg once daily. To treat erosive esophagitis DELAYED-RELEASE , DELAYED-RELEASE SUSPENSION, DELAYED-RELEASE ORALLY

Adults.Initial: 30 mg daily before morning meal for up to 8 wk. Continued another 8 wk if indicated. Maintenance: 15 mg daily. To treat erosive esophagitis short-term (up to 7 days) in patients unable to take oral medication
IV:
Adults.30 mg daily infused over 30 min for up to 7 days. To treat pathological hypersecretory conditions, such as Zollinger-Ellison syndrome DELAYED-RELEASE , DELAYED-RELEASE SUSPENSION, DELAYED-RELEASE ORALLY

Adults. Initial: 60 mg daily before morning meal, increased as needed according to patient’s condition. Doses exceeding 120 mg/day administered in divided doses. Maximum: 180 mg daily. To eradicate Helicobacter pylori and reduce risk of duodenal ulcer recurrence DELAYED-RELEASE , DELAYED-RELEASE SUSPENSION, DELAYED-RELEASE ORALLY

Adults.30 mg plus 1 g amoxicillin and 500 mg clarithromycin every 12 hr before meals for 10 to 14 days. Or, 30 mg plus 1 g amoxicillin t.i.d. before meals for 14 days. To treat symptomatic pediatric gastroesophageal reflux disease DELAYED-RELEASE , DELAYED-RELEASE SUSPENSION, DELAYED-RELEASE ORALLY
Children ages 12 to 17. 15 mg daily for up to 8 wk. Children ages 1 to 11 weighing 30 kg (66 lb) or less. 15 mg daily for up to 12 wk. Children ages 1 to 11 weighing more than 30 kg.30 mg daily for up to 12 wk. To treat symptomatic pediatric erosive esophagitis DELAYED-RELEASE , DELAYED-RELEASE SUSPENSION, DELAYED-RELEASE ORALLY
Children ages 12 to 17. 30 mg daily for up to 8 wk. Children ages 1 to 11 weighing 30 kg (66 lb) or less. 15 mg daily for up to 12 wk. Children ages 1 to 11 weighing more than 30 kg. 30 mg daily for up to 12 wk. To treat frequent heartburn (PREVACID24-HR)
Adults. 1 capsule daily for 14 days. May repeat course every 4 months. Route Onset Peak Duration P.O. 1–3 hr Unknown Over 24 hr

Mechanism of Action

Binds to and inactivates the hydrogenpotassium adenosine triphosphate enzyme system (also called the proton pump) in gastric parietal cells. This action blocks the final step of gastric acid production.

Incompatibilities

Don’t give any other with parenteral lansoprazole, and dilute only with solutions recommended by manufacturer (sterile water for initial reconstitution and normal saline solution, lactated Ringer’s solution, or D5W for further dilution).

Contraindications

Hypersensitivity to lansoprazole or its components

Interactions

ampicillin, digoxin, iron salts, ketoconazole, other that depend on low gastric pH for bioavailability: Inhibited absorption of these atazanavir: Decreased blood level and possibly reduced effectiveness of atazanavir sucralfate: Delayed lansoprazole absorption
theophylline: Slightly decreased blood theophylline level
warfarin: Increased INR and PT with possibly increased risk of serious bleeding

Side Efect

CNS: Dizziness, headache
GI: Abdominal pain, anorexia, diarrhea, elevated liver enzymes, hepatotoxicity, increased appetite, nausea, pancreatitis, pseudomembranous colitis, vomiting
GU: Interstitial nephritis, urine retention
HEME: Agranulocytosis, aplastic anemia, decreased hemoglobin, hemolytic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia, thrombotic thrombocytopenic purpura
MS: Arthralgia, myositis
RESP: Upper respiratory tract infection
SKIN: Erythema multiforme, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, hyperkalemia, injection site reaction

Cautions

Give lansoprazole before meals. Antacids may be given as well, if needed.

If patient is prescribed capsules and has trouble swallowing them, open and sprinkle granules on applesauce, Ensure, pudlansoprazole 570 ding, cottage cheese, yogurt, or strained pears. Don’t crush granules. Have patient swallow mixture immediately. Or, empty granules into 2 ounces apple, orange, or tomato juice; mix quickly, and have patient swallow immediately. Then add 2 or more ounces of juice to glass and have patient drink immediately to ensure full dose.

For delayed-release orally disintegrating tablets, place tablet on patient’s tongue and let it dissolve, with or without water, until patient can swallow particles.

For patient with nasogastric tube, don’t use oral suspension. Instead use capsules or orally
. For capsule form, open capsule, mix granules in 40 ml apple juice only, and inject through tube. Then flush tube with apple juice only. For
, place tablet in syringe and draw up 4 ml (for 15-mg tablet) or 8 ml (for 30-mg tablet) of water. Shake gently, and inject through tube within 15 minutes. Then refill syringe with 5 ml of water, shake gently, and inject through tube.

For delayed-release oral suspension, empty packet contents into a container with 2 tablespoons water (no other liquids or ), stir well, and have patient drink immediately. If any particles remain in container, add more water, stir, and have patient drink again immediately.

Reconstitute parenteral form by injecting 5 ml sterile water into 30-mg drug vial. Mix gently until powder dissolves. Use within 1 hour. After reconstitution, dilute with 50 ml normal saline solution, lactated Ringer’s solution, or D5W. Give within 12 hours if mixed with D5W or 24 hours if mixed with normal saline solution or lactated Ringer’s solution.

Give parenteral drug with a filter following manufacturer’s guidelines. Change filter every 24 hours. Give as I.V. infusion over 30 minutes. Flush line with normal saline solution, lactated Ringer’s solution, or D5W before and after giving lansoprazole.

Expect to give lansoprazole with antibiotics because decreased gastric acid secretion helps antibiotics eradicate H. pylori.

If lansoprazole is given with antibiotics, watch for diarrhea from possible pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold drug and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

PATIENT SAFTY

Urge patient to take drug exactly as prescribed, usually before a meal (preferably breakfast) to decrease gastric acid output.

If patient has trouble swallowing dexlansoprazole capsules, tell her to open them and sprinkle granules on 1 tablespoon of applesauce and swallow immediately. If patient has trouble swallowing lansoprazole capsules, tell her to open them and sprinkle granules on applesauce, Ensure, pudding, cottage cheese, yogurt, or strained pears and to swallow immediately without chewing. Or, she may empty granules into 2 ounces of apple, orange, or tomato juice, mix quickly, and swallow immediately. Tell her to refill glass with 2 or more ounces of juice and drink immediately to ensure a full dose.

If patient was prescribed delayed-release orally
, tell her to place tablet on tongue, let it dissolve, and then swallow particles with or without water.

If patient was prescribed delayed-release oral suspension, tell her to empty contents of packet into a container with 2 tablespoons of water (no other liquids or ), stir well, and drink immediately. If particles remain in container, she should add water, stir, and drink immediately.

Inform patient that she may take antacids with lansoprazole.

Advise patient to report severe headache, or worsening of symptoms immediately to prescriber.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and can be serious, requiring prompt treatment.

Category

Chemical class: Rare earth element
Therapeutic class: Phosphate binder

Pregnancy category: C

Indications

To reduce serum phosphate levels in patients with end-stage renal disease
Adults. Initial: 250 to 500 mg t.i.d. with meals; increased, as needed, by 750 mg daily every 2 to 3 wk until acceptable serum phosphate level is reached.

Contraindications

Bowel obstruction, hypersensitivity to lanthanum carbonate or any of its components, hypophosphatemia

Side Efect

CNS: Headache
CV: Hypotension
EENT: Rhinitis
ENDO: Hypercalcemia
GI: Abdominal pain, constipation, diarrhea, nausea, vomiting
GU: Dialysis graft occlusion
RESP: Bronchitis

Cautions

Use lanthanum carbonate cautiously in patients with acute peptic ulcer, ulcerative colitis, Crohn’s disease, or bowel obstruction because drug effects are unknown in these patients.

Monitor the patient’s serum phosphate levels, as ordered, especially during dosage adjustment, to determine effectiveness of lanthanum carbonate therapy. Serum phosphate levels should fall below 6.0 mg/dl.

PATIENT SAFTY

Instruct patient to take lanthanum carbonate with or immediately after meals.

Advise patient to chew each tablet thoroughly before swallowing. If patient has trouble chewing tablets, tell her she may crush them.

Urge patient to take drug exactly as prescribed, and explain that it may take weeks to reach a desired serum phosphate level.

Category

Chemical class: Malonitrilamide immunomodulator
Therapeutic class: Antirheumatic

Pregnancy category: X

leflunomide 572 Duodenum cross section Duodenum cross section Phosphate molecule Phosphate molecule Villi Villi Insoluble phosphate Released lanthanum ion Duodenum cross section Duodenum cross section Phosphate molecule Phosphate molecule Villi Villi Insoluble phosphate Released lanthanum ion

Mechanism of Action

During digestion, phosphate is released into the upper GI tract (below left) and absorbed into the bloodstream, increasing serum phosphate levels. In patients with end-stage renal disease, however, inefficient phosphate clearance from the blood leads to abnormally elevated levels. Lanthanum dissociates in the upper GI tract, releasing ions that attach to unbound phosphate to form an insoluble complex (below right). Unabsorbed into the bloodstream, these altered phosphate molecules can’t elevate the patient’s serum phosphate level.

Indications

To relieve symptoms of active rheumatoid arthritis, improve physical function and slow disease progression
Adults. Loading: 100 mg daily for 3 days. Maintenance: 20 mg daily, reduced to 10 mg daily if poorly tolerated. Maximum: 20 mg/ day.

Mechanism of Action

Inhibits dihydroorotate dehydrogenase, the enzyme in autoimmune process that leads to rheumatoid arthritis. With this action, leflunomide relieves inflammation and prevents alteration of the autoimmune process.

Contraindications

Hypersensitivity to leflunomide or its components, pregnancy

Interactions

activated charcoal, cholestyramine: Decreased blood leflunomide level live-virus vaccines: Possibly adverse reactions to vaccines caused by leflunomideinduced immunosuppression methotrexate: Risk of hepatotoxicity
NSAIDs: Possibly impaired NSAID metabolism rifampin, tolbutamide: Increased blood leflunomide level

Side Efect

CNS: Anxiety, dizziness, drowsiness, fatigue, fever, headache, paresthesia
CV: Chest pain, hypertension, palpitations, tachycardia
EENT: Blurred vision, conjunctivitis, dry mouth, epistaxis, mouth ulcers, pharyngitis, rhinitis, sinusitis
GI: Abdominal pain, cholestasis, constipation, diarrhea, elevated liver function test results, flatulence, gastritis, gastroenteritis, hepatic failure, hepatitis, nausea, vomiting
GU: UTI
HEME: Agranulocytosis, anemia, pancytopenia, thrombocytopenia
MS: Back pain, synovitis, tendinitis
RESP: Asthma, bronchitis, dyspnea, interstitial lung disease, respiratory tract infection
SKIN: Alopecia (transient), erythematous rash, jaundice, pruritus, urticaria
Other: Sepsis, weight loss

Cautions

Leflunomide isn’t recommended for patients with severe immunodeficiency, bone marrow dysplasia, or severe, uncontrolled infections because of its immunosuppressant effect.

Test patient for latent tuberculosis before starting leflunomide. If positive, expect standard medical treatment to be given before leflunomide therapy starts.

Obtain baseline blood pressure before starting leflunomide, and monitor periodically thereafter because drug may cause hypertension.

Assess liver enzyme (ALT and AST) levels at start of therapy, monthly during first 6 months, and if stable, every 6 to 8 weeks thereafter, as ordered. Expect to stop drug if hepatic dysfunction develops.

Obtain platelet count, WBC count, and hemoglobin or hematocrit at start of therapy and every 4 to 8 weeks thereafter, as ordered.

Notify prescriber if patient develops serious infection because drug may need to be interrupted and cholestyramine or charcoal given to eliminate drug rapidly.
WARNING Monitor patient’s respiratory function closely because drug may cause interstitial lung disease that could become life-threatening. If patient develops a cough and dyspnea, notify prescriber; drug may need to be stopped, and patient may need cholestyramine or charcoal to eliminate drug rapidly.

PATIENT SAFTY

Advise patient that leflunomide doesn’t cure arthritis but may relieve its symptoms and improve physical function.

Inform patient that reversible hair loss may occur.

Caution woman of childbearing potential not to become pregnant while taking drug because of the high risk of birth defects.

Instruct patient to report signs of hepatotoxicity, such as mouth ulcers, unusual bleeding or bruising, and yellow skin or eyes.

Tell patient to report signs of respiratory dysfunction, such as cough and dyspnea.

Advise patient to avoid live vaccines during leflunomide therapy.

Instruct patient to notify prescriber if she develops an infection.

Category

Chemical class: Yeast-derived recombinant form of hirudin
Therapeutic class: Anticoagulant

Pregnancy category: B

Indications

To prevent thromboembolic complications in patients with heparin-induced thrombocytopenia and associated thromboembolic disease
IV: AND INJECTION
Adults. Initial: 0.4 mg/kg, but no more than 44 mg, given by bolus over 15 to 20 sec, followed by continuous infusion of 0.15 mg/ kg/hr for 2 to 10 days or longer, as indicated. Maximum: 0.21 mg/kg/hr.
DOSAGE ADJUSTMENT For patients with renal insufficiency, bolus dose decreased to 0.2 mg/kg and infusion rate adjusted as follows: for creatinine clearance of 45 to 60 ml/ min/1.73 m2, 50% of standard infusion rate; for clearance of 30 to 44 ml/min/ 1.73 m2, 30% of standard infusion rate; for clearance of 15 to 29 ml/min/1.73 m2, 15% of standard infusion rate; for clearance less than 15 ml/min/1.73 m2, expect drug to be stopped. Route Onset Peak Duration I.V. Immediate Unknown Unknown

Mechanism of Action

Forms a tight bond with thrombin, neutralizing this enzyme’s actions, even when the enzyme is trapped within clots. One molecule of lepirudin binds with one molecule of thrombin. Thrombin causes fibrinogen to convert to fibrin, which is essential for clot formation.

Incompatibilities

Don’t mix lepirudin in same I.V. line with other .

Contraindications

Hypersensitivity to lepirudin or other hirudins

Interactions

oral anticoagulants, platelet aggregation inhibitors, thrombolytics: Increased risk of bleeding complications and enhanced effects of lepirudin

Side Efect

CNS: Chills, fever, intracranial hemorrhage
CV: Heart failure
EENT: Epistaxis
GI: GI or rectal bleeding, hepatic dysfunction
GU: Hematuria, vaginal bleeding
HEME: Anemia, easy bruising, hematoma
RESP: Hemoptysis, pneumonia
SKIN: Excessive bleeding from wounds, rash, pruritus, urticaria
Other: Anaphylaxis, injection site bleeding, sepsis

Cautions

Be aware that patients with heparininduced thrombocytopenia have low platelet counts, which can lead to severe bleeding and even death. Lepirudin works to prevent clotting without further reducing platelet count.

To reconstitute, mix lepirudin with normal saline solution or sterile water for injection. Warm solution to room temperature before giving.

For I.V. bolus delivery, reconstitute 50 mg drug with 1 ml sterile water for injection or sodium chloride for injection. Then further dilute by withdrawing reconstituted solution into 10-ml syringe and adding enough sterile water for injection, sodium chloride for injection, or D5W to produce a total volume of 10 ml, or 5 mg of lepirudin/ml. Administer prescribed dose over 15 to 20 seconds.

For I.V. infusion, reconstitute 2 vials of drug and transfer to infusion bag that contains 250 or 500 ml normal saline solution or D5W. Concentration will be 0.4 or 0.2 mg/ml.

Adjust infusion rate as prescribed, according to patient’s APTT ratio, which is APTT divided by a control value. Target APTT ratio during treatment is 1.5 to 2.5.

Expect to obtain first APTT 4 hours after starting infusion and to obtain follow-up APTT daily (more often for patients with hepatic or renal impairment).

Stop infusion for 2 hours, as ordered, if APTT is above target range. Expect to decrease infusion rate by half when relepirudin 574 starting. If APTT is below target range, expect to increase rate in 20% increments and recheck APTT in 4 hours.

Avoid I.M. injections or needle sticks during lepirudin therapy to minimize risk of hematoma.

Observe I.M. injection sites, I.V. infusion sites, and wounds for bleeding.

Monitor patient for ecchymoses on arms and legs, epistaxis, hematemesis, hematuria, melena, and vaginal bleeding.

Be aware that when patient is scheduled to switch to an oral anticoagulant, lepirudin dosage may need to be tapered over a period of days, as ordered, until APTT is just above 1.5, before starting oral anticoagulant. In addition, INR and PT will need to be monitored closely, as ordered, to prevent bleeding adverse effects.

PATIENT SAFTY

Tell patient to report unexpected bleeding, such as blood in urine, easy bruising, nosebleeds, tarry stools, and vaginal bleeding.

Advise patient to avoid bumping arms and legs because of the risk of bruising.

Instruct patient to use electric razor and soft toothbrush to reduce risk of bleeding.

Category

Chemical class: Synthetic peptide gonadotropin-releasing hormone analogue
Therapeutic class: Antianemic, antiendometrionic agent, antineoplastic, gonadotropin inhibitor

Pregnancy category: X

Indications

To treat prostate cancer
I.M.INJECTION(LEUPROLIDE ACETATE FOR INJECTION)
Adults.7.5 mg/mo, 22.5 mg every 3 mo, or 45 mg every 4 mo. SUBCUTANEOUS INJECTION(LEUPROLIDE ACETATE FOR INJECTABLE SUSPENSION)
Adults. 7.5 mg/mo. SUBCUTANEOUS INJECTION(LEUPROLIDE ACETATE INJECTION)
Adults. 1 mg daily. To provide palliative treatment of advanced prostate cancer SUBCUTANEOUS INJECTION(ELIGARD FOR INJECTABLE SUSPENSION)
Adults.7.5 mg/mo. 22.5 mg every 3 mo, or 45 mg every 6 mo. To treat precocious central puberty
I.M.INJECTION(LEUPROLIDE ACETATE FOR INJECTION) Children weighing more than 37.5 kg (83 lb). Initial: 15 mg every 4 wk. Maintenance: Dosage increased as needed in increments of 3.75 mg every 4 wk. Maximum: 15 mg every 4 wk. Children weighing 25 to 37.5 kg (55 to 83 lb). Initial: 11.25 mg every 4 wk. Maintenance: Dosage increased as needed in increments of 3.75 mg every 4 wk. Maximum: 15 mg every 4 wk. Children weighing less than 25 kg. Initial: 7.5 mg every 4 wk. Maintenance: Dosage increased as needed in increments of 3.75 mg every 4 wk. Maximum: 15 mg every 4 wk. SUBCUTANEOUS INJECTION(LEUPROLIDE ACETATE INJECTION) Children.50 mcg/kg daily. Dosage increased in increments of 10 mcg/kg daily. To treat endometriosis
I.M.INJECTION(LEUPROLIDE ACETATE FOR INJECTION)
Adults. 3.75 mg every mo or 11.25 mg every 3 mo for up to 6 mo. Maximum: 33.75 mg total dose. As adjunct to treat anemia due to uterine leiomyomas
I.M.INJECTION(LEUPROLIDE ACETATE FOR INJECTION)
Adults. 3.75 mg every mo up to 3 mo or 11.25 mg single dose. Maximum: 11.25 mg total dose.

Mechanism of Action

After stimulating follicle-stimulating hormone (FSH) and luteinizing hormone (LH), continuous leuprolide therapy suppresses secretion of gonadotropin-releasing hormone, decreasing testosterone and estradiol levels. In children with central precocious puberty, this stops menses and reproductive organ development. leuprolide acetate 575 J K L In adult men, continuous suppression decreases testosterone levels and causes pharmacologic castration, which slows the activity of prostatic neoplastic cells. In women with endometriosis or uterine leiomyomas, leuprolide suppresses ovarian function, inactivating endometrial tissues and resulting in amenorrhea. Route Onset Peak Duration I.M., 1 wk Unknown 4–12 wk SubQ* after therapy I.M., 2–4 wk After 1– 60–90 SubQ 2 mo days after therapy

Contraindications

Women and children (leuprolide acetate injectable suspension); hypersensitivity to benzyl alcohol, gonadorelin, and gonadotropin-releasing hormone analogues, including leuprolide, and their components; pregnancy; undiagnosed abnormal vaginal bleeding

Side Efect

CNS: Depression, dizziness, fatigue, headache, insomnia, lethargy, malaise, memory loss, paresthesia, peripheral neuropathy, rigors, seizures, syncope, weakness; anxiety, mood changes, nervousness (adult women)
CV: Arrhythmias, edema, hypertension, hypotension, palpitations, vasodilation; angina, MI, thrombophlebitis (adult men)
EENT: Blurred vision
ENDO: Amenorrhea, androgenic effects in women. breast tenderness or swelling, decreased testicle size, gynecomastia, hot flashes, hyperglycemia, pituitary apoplexy
GI: Colitis, constipation in adult men, dyspepsia, gastroenteritis, hepatic dysfunction, nausea, vomiting
GU: Bladder spasm, decreased libido, decreased penis size, dysuria, endometriosis flareup, impotence, incontinence, nocturia, prostate cancer flareup, prostate pain, uterine bleeding, vaginal discharge in girls, vaginitis
HEME: Leukopenia
MS: Arthralgia, body pain in children, bone density loss, bone or limb pain, fibromyalgia, myalgia, tenosynovitis
RESP: Asthma, dyspnea, pulmonary embolism
SKIN: Alopecia, clamminess, night sweats, photosensitivity, rash, urticaria
Other: Anaphylaxis; weight gain; injection site abscess, burning, edema, induration, itching, pain, or redness

Cautions

Let drug come to room temperature before using. Reconstitute leuprolide acetate depot suspension with diluent provided by manufacturer. Add diluent to powder for suspension and thoroughly shake vials to disperse particles into a uniform milky suspension. Use within 30 minutes after mixing, and discard any unused portion. If using a prefilled dualchamber syringe, follow manufacturer’s instructions to release diluent into chamber containing powder. Shake gently after diluted to disperse particles evenly in solution. No dilution or reconstitution is needed for leuprolide acetate injection for subcutaneous administration. Rotate injection sites.
WARNING Leuprolide acetate for injectable suspension (Eligard) is approved only for use in men for palliative treatment of prostate cancer. Use provided syringes and delivery system, and read and follow instructions carefully to ensure proper mixing of product; shaking alone is inadequate to mix it.
WARNING Monitor patient for possible allergic reaction (erythema and induration) at injection site because leuprolide injections contain benzyl alcohol. Manufacturer recommends that injection be given by physician.

During first weeks of leuprolide therapy, monitor patient being treated for prostate cancer for initial worsening of symptoms, such as increased bone pain, difficult urination, and paresthesia or paralysis (in patients with vertebral metastasis).

During treatment for prostate cancer, monitor patient’s serum testosterone and PSA levels periodically, as ordered, to determine response to leuprolide therapy.

Expect to stop drug before age 11 in female patients and age 12 in male leuprolide acetate 576 *Gonadotropin inhibitor. Antiendometrionic, antineoplastic. patients treated for precocious central puberty.

Monitor bone density test results, as ordered, of women at risk for osteoporosis who are receiving leuprolide because of possible drug-induced estrogen loss, which may result in decreased bone density.

Be aware that therapeutic doses of leuprolide suppress the pituitary-gonadal system and that normal function doesn’t return for 4 to 12 weeks after drug is stopped.
WARNING Monitor patient for evidence of pituitary apoplexy, such as sudden headache, vomiting, visual changes, ophthalmoplegia, altered mental status, and possibly cardiovascular collapse. Although rare, it may occur within 2 weeks of first dose, sometimes within the first hour. Notify prescriber immediately and provide supportive care.

PATIENT SAFTY

Instruct patient who is self-administering leuprolide injection to use syringe provided by manufacturer. If manufacturer’s syringe is unavailable, advise her to use only a 0.5-ml disposable, low-dose, U-100 insulin syringe to ensure accurate dosage. Substitution of syringes is not recommended for leuprolide acetate for injectable suspension.

Advise women to immediately report monthly menses or breakthrough bleeding to prescriber.

Instruct female patient of childbearing age to use a nonhormonal form of contraception during leuprolide therapy. Advise her to stop taking drug and notify prescriber at once if she becomes pregnant.

Inform patient with osteoporosis or at risk for developing it that drug may increase bone density loss.

Inform parents of child being treated for central precocious puberty that they should expect normal gonadal-pituitary function to return 4 to 12 weeks after therapy ends.

Advise patient to report symptoms of depression or memory problems.

Caution patient being treated for prostate cancer that drug may initially worsen such symptoms as bone pain and that it may cause new signs or symptoms to occur during first few weeks of treatment. Reassure patient that this is transient.

Category

Chemical class: Sympathomimetic amine
Therapeutic class: Bronchodilator

Pregnancy category: C

Indications

To prevent or treat bronchospasm in reversible obstructive airway disease INHALATION AEROSOL Adults and children age 4 and over. 45 or 90 mcg (1 or 2 inhalations) every 4 to 6 hr. INHALATION SOLUTION Adults and children age 12 and over. 0.63 to 1.25 mg t.i.d. every 6 to 8 hr. Maximum: 1.25 mg t.i.d. Children ages 6 to 11. 0.31 to 0.63 mg t.i.d. Maximum: 0.63 mg t.i.d.
DOSAGE ADJUSTMENT For elderly patients, dosage limited to 0.63 mg t.i.d. every 6 to 8 hr. Route Onset Peak Duration Inhalation 10–17 min 1.5 hr 5–6 hr

Mechanism of Action

Attaches to beta2receptors on bronchial cell membranes, which stimulates the intracellular enzyme adenyl cyclase to convert adenosine triphosphate to cAMP. Increased intracellular cAMP level relaxes bronchial smooth muscle and inhibits histamine release from mast cells.

Contraindications

Hypersensitivity to levalbuterol, other sympathomimetic amines, or their components

Interactions

beta blockers: Blocked effects of both digoxin: Decreased blood digoxin level loop or thiazide diuretics: Increased risk of hypokalemia MAO inhibitors, sympathomimetics, tricyclic antidepressants: Increased risk of adverse cardiovascular effects

Side Efect

CNS: Anxiety, chills, dizziness, hypertonia, levalbuterol hydrochloride 577 J K L insomnia, migraine headache, nervousness, paresthesia, syncope, tremor
CV: Chest pain, hypertension, hypotension, tachycardia
EENT: Dry mouth and throat, rhinitis, sinus-itis
GI: Diarrhea, indigestion, nausea, vomiting
MS: Leg cramps, myalgia
RESP: Asthma exacerbation, cough, dyspnea, paradoxical bronchospasm
Other: Flulike symptoms, lymphadenopathy

Cautions

Use levalbuterol cautiously in patients with arrhythmias, diabetes mellitus, hypertension, hyperthyroidism, or a history of seizures.

Give oral solution form only by nebulizer.

Monitor pulse rate and blood pressure before and after nebulizer treatment.

Because drug may provoke paradoxical bronchospasm, observe for dyspnea, wheezing, and increased coughing.

PATIENT SAFTY

Teach patient how to use levalbuterol nebulizer and to measure correct dose.

Intsruct patient to prime inhaler before using it for the first time or when it hasn’t been used for more than 3 days by releasing 4 test sprays into the air, aiming it away from her face.

Show patient how to clean nebulizer or inhaler, and explain the need to do so at least once weekly.

Instruct patient to notify prescriber if drug fails to work or if she needs more treatments because asthma is worsening.

Instruct patient not to increase dosage or frequency unless told by prescriber.

Urge patient to stop drug and call prescriber if she has paradoxical bronchospasm.

Instruct patient to use inhalation solution within 2 weeks of opening the foil pouch and to protect drug from light and heat.

Urge patient to consult prescriber before using OTC or other .

Category

Chemical: Pyrrolidine derivative
Therapeutic: Anticonvulsant

Pregnancy category: C

Indications

As adjunct to treat partial seizures

ORALL

, Adults and adolescents over age 16. Initial: 500 mg b.i.d., increased by 1,000 mg daily every 2 wk if needed. Maximum: 3,000 mg daily. Children ages 4 to 16. Initial: 10 mg/kg b.i.d., increased by 20 mg/kg daily every 2 wk until recommended daily dose of 60 mg/kg is reached. XR Adults and adolescents over age 16. 1,000 mg once daily, increased by 1,000 mg daily every 2 wk until recommended daily dose of 3,000 mg is reached.
IV: Adults and adolescents over age 16. Initial: 500 mg infused over 15 minutes b.i.d., increased by 1,000 mg daily every 2 wk, if needed. Maximum: 3,000 mg daily. As adjunct to treat myoclonic seizures in patients with juvenile myoclonic epilepsy

ORALL

, Adults and children age 12 and over. Initial: 500 mg b.i.d., increased by 1,000 mg daily every 2 wk, if needed. Maximum: 3,000 mg daily. As adjunct to treat primary generalized tonic-clonic seizures in patients with idiopathic generalized epilepsy

ORALL

, Adults and children age 6 and over. Initial: 500 mg b.i.d., increased by 1,000 mg daily every 2 wk, as needed. Maximum: 3,000 mg daily.
DOSAGE ADJUSTMENT Maximum dosage reduced to 2,000 mg daily for patients with creatinine clearance of 50 to 80 ml/min/ 1.73 m2; to 1,500 mg daily for clearance of 30 to 49 ml/min/1.73 m2; and to 1,000 mg daily for clearance less than 30 ml/min/ 1.73 m2. For patients with end-stage renal disease who are having dialysis, expect to give another 250 to 500 mg, as prescribed, after each dialysis session. For children who can’t tolerate 60 mg/kg daily, dosage reduced to point of tolerance.

Mechanism of Action

May protect against secondary generalized seizure activity by preventing coordination levetiracetam 578 of epileptiform burst firing. Levetiracetam doesn’t seem to involve inhibitory and excitatory neurotransmission.

Contraindications

Hypersensitivity to levetiracetam or its components

Side Efect

CNS: Abnormal gait, aggression, agitation, anger, anxiety, apathy, asthenia, ataxia, behavioral difficulties (children), confusion, coordination difficulties, depersonalization, depression, dizziness, emotional lability, fatigue, hallucinations, headache, hostility, increased reflexes, insomnia, irritability, mental or mood changes, nervousness, neurosis, paresthesia, personality disorder, psychosis, seizures, somnolence, suicidal ideation, vertigo
EENT: Amblyopia, conjunctivitis, diplopia, ear pain, nasopharyngitis, pharyngitis, rhinitis, sinusitis
GI: Anorexia, constipation, diarrhea, elevated liver enzyme levels, gastroenteritis, hepatic failure, hepatitis, pancreatitis, vomiting
GU: Albuminuria
HEME: Decreased hemtatocrit, hemoglobin, and total mean RBC count; leukopenia; neutropenia; pancytopenia; thrombocytopenia
MS: Neck pain
RESP: Asthma, cough
SKIN: Alopecia, ecchymosis, pruritus, skin discoloration, vesiculobullous rash
Other: Dehydration, facial edema, infection, influenza, weight loss

Cautions

Children weighing 20 kg or less should be given only the oral solution form.

For I.V. use, dilute parenteral levetiracetam in 100 ml of compatible diluent, such as normal saline injection, lactated Ringer’s injection, or dextrose 5% injection. Use within 24 hours.

Assess compliance during first 4 weeks of therapy, when

Side Efect

are most common.

Monitor patient for seizure activity during therapy. As appropriate, implement seizure precautions according to facility policy.

Stopping drug may increase seizure activity. Expect to taper dosage gradually.

Certain adverse effects, including somnolence, fatigue, coordination problems, and abnormal behaviors may be more likely in patieints taking levetiracetam for partial seizure disorders.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

PATIENT SAFTY

Caution patient that levetiracetam may cause dizziness and drowsiness, especially during first 4 weeks of therapy.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Caution patient not to stop taking levetiracetam abruptly; inform her that drug dosage should be tapered under prescriber’s direction to reduce the risk of breakthrough seizures.

Explain that levetiracetam may cause mental and behavioral changes, such as aggression, depresison, irritability, and rarely psychotic symptoms. Urge her to contact prescriber about any bothersome changes.

Advise patient to keep taking other anticonvulsants, as ordered, while taking levetiracetam.

Encourage patient to avoid alcohol during therapy because alcohol can increase incidence of drowsiness and dizziness.

Instruct patient to see prescriber regularly so that her progress can be monitored.

Urge caregivers to watch patient closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes, and to report concerns immediately.

Urge woman who becomes pregnant while taking levetiracetam to enroll in the North American antiepileptic drug pregnancy registry by calling 1-888-233-2334. Explain that registry is collecting information about safety of antiepileptic during pregnancy.

Category

Chemical class: H1-receptor antagonist
Therapeutic class: Antihistamine

Pregnancy category: B

levocetirizine 579 J K L

Indications

To treat chronic idiopathic urticaria; to treat allergic rhinitis , Adults and children age 12 and over. 2.5 to 5 mg once daily in evening. Maximum: 5 mg daily.
DOSAGE ADJUSTMENT For patient with mild renal impairment (creatinine clearance 50 to 80 ml/min/1.73 m2), dosage shouldn’t exceed 2.5 mg daily. For patient with moderate renal impairment (creatinine clearance 30 to 50 ml/min/1.73 m2), dosage shouldn’t exceed 2.5 mg once every other day. For patient with severe renal impairment (creatinine clearance 10 to 30 ml/ min/1.73 m2), dosage shouldn’t exceed 2.5 mg once every 3 to 4 days. Children ages 6 to 11. 2.5 mg once daily in evening. Maximum: 2.5 mg daily.

Mechanism of Action

Binds to central and peripheral H1receptors, competing with histamine for these sites and preventing it from reaching its site of action. By blocking histamine, levocetirizine produces antihistamine effects, inhibiting respiratory, vascular, and GI smooth-muscle contraction; decreasing capillary permeability, which reduces wheals, flares, and itching; and decreasing salivary and lacrimal gland secretions to relieve chronic urticaria and signs and symptoms of allergic rhinitis.

Contraindications

Children ages 6 to 11 with impaired renal function; creatinine clearance less than 10 ml/min/1.73 m2; end-stage renal disease in adults and children age 12 and over; hypersensitivity to levocetirizine, cetirizine or their components; renal failure

Interactions

CNS depressants: Possibly increased CNS depression
MAO inhibitors: Possibly prolonged and intensified anticholinergic effects ritonavir: Possibly increased risk of adverse effects of levocetirizine
theophylline: Possibly decreased clearance of levocetirizine
alcohol use: Possibly increased CNS depression

Side Efect

CNS: Aggression, agitation, asthenia, fatigue, fever, seizures, somnolence, syncope
CV: Palpitations
EENT: Dry mouth, epistaxis, nasopharyngitis, pharyngitis, visual disturbances
GI: Hepatitis, nausea
MS: Myalgia
RESP: Cough, dyspnea
SKIN: Pruritus, rash, urticaria
Other: Anaphylaxis, angioedema, weight gain

Cautions

Expect to stop drug at least 72 hours before skin tests for allergies because drug may inhibit cutaneous histamine response, thus producing false-negative results.

PATIENT SAFTY

Instruct patient to take drug exactly as prescribed. For oral solution, patient should use appropriate measuring device.

Urge patient to avoid alcohol while taking levocetirizine

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Category

Chemical class: Dihydroxyphenylalanine isomer, metabolic precursor of dopamine
Therapeutic class: Antidyskinetic

Pregnancy category: Not rated

Indications

To manage symptoms of primary Parkinson’s disease, postencephalitic parkinsonism, and parkinsonism caused by CNS injury from carbon monoxide or manganese intoxication , Adults and children age 12 and over. Initial: 250 mg daily in divided doses b.i.d. to q.i.d. Increased by 100 to 750 mg every 3 to 7 days, as indicated. Maximum: 8 g daily.

Contraindications

Angle-closure glaucoma, history of melanoma, hypersensitivity to levodopa or its components, suspicious undiagnosed skin levodopa 580 lesions, use within 14 days of MAO inhibitor therapy Route Onset Peak Duration P.O. 14–21 days* Unknown 5 hr

Interactions

antacids: Increased blood levodopa level antihypertensives: Risk of orthostatic hypotension benzodiazepines: Possibly decreased therapeutic effects of levodopa bromocriptine: Possibly additive effects of levodopa furazolidone, MAO inhibitors, procarbazine: Risk of severe hypertension haloperidol, loxapine, molindone, papaverine, phenothiazines, phenytoin, rauwolfia alkaloids: Decreased effects of levodopa inhaled anesthetics, sympathomimetics: Increased risk of arrhythmias iron salts: Possibly decreased blood level and effectiveness of levodopa methyldopa: Possibly toxic CNS effects metoclopramide: Possibly worsening of Parkinson’s disease and decreased therapeutic effects of metoclopramide pyridoxine (vitamin B6): Decreased antidyskinetic effect of levodopa high-protein food: Decreased levodopa absorption cocaine use: Increased risk of arrhythmias

Side Efect

CNS: Aggressiveness, anxiety, ataxia, confusion, delusions, dizziness, dream disturbances, dyskinesia, dystonia, euphoria, hallucinations, headache, increased tremor, insomnia, malaise, mood changes, severe depression, suicidal tendencies, syncope, weakness
CV: Arrhythmias, hot flashes, orthostatic hypotension, palpitations
EENT: Bitter aftertaste, blurred vision, darkened saliva, diplopia, dry mouth, increased salivation, mydriasis, tooth clenching and grinding levodopa 581 J K L D2 receptor Postsynaptic neuron Basal ganglion neuron Dopamine Levodopa

Mechanism of Action

By supplementing a low level of endogenous dopamine, levodopa helps control alterations in voluntary muscle movement (such as tremors and rigidity) in Parkinson’s disease. Dopamine, a neurotransmitter synthesized and released by neurons leading from substantia nigra to basal ganglia, is essential for normal motor function. By stimulating peripheral and central dopaminergic2(D2) receptors on postsynaptic cells, dopamine inhibits the firing of striatal neurons (such as cholinergic neurons). In Parkinson’s disease, progressive degeneration of these neurons substantially reduces the supply of intrasynaptic dopamine. Levodopa, a dopamine precursor, increases the dopamine supply in neurons, making more available to stimulate dopaminergic receptors. * With multiple doses.
GI: Abdominal pain, anorexia, constipation, diarrhea, flatulence, GI bleeding, hepatotoxicity, hiccups, indigestion, nausea, vomiting
GU: Darkened urine, priapism, urine retention
SKIN: Darkened sweat, diaphoresis, rash

Cautions

Expect to discontinue levodopa 6 to 8 hours before surgery to avoid interactions with anesthetics.

Observe patient for mental or behavioral changes and suicidal tendencies. Notify prescriber immediately if they occur.

Watch for muscle twitching and blepharospasm (eyelid spasm), which are early signs of levodopa overdose. Report them at once.

Expect patient to be tested for acromegaly and diabetes during long-term levodopa therapy. Also expect to monitor hematopoietic, hepatic, and renal function.

PATIENT SAFTY

Advise patient to take levodopa with meals if she experiences adverse GI reactions.

Because protein impairs drug absorption, instruct patient to avoid high-protein meals during levodopa therapy and to distribute protein intake equally throughout the day.

Caution patient to avoid excessive use of vitamins and fortified cereals that contain vitamin B6or iron, which can reduce levodopa’s effects.

Instruct patient to report fainting,increased muscle tremor, difficult urination, and severe or persistent nausea and vomiting.

Urge patient to continue taking drug as prescribed even if results of therapy aren’t evident immediately.

Inform patient that saliva, sweat, and urine may darken but that this isn’t harmful.

Direct patient to protect drug from heat, light, and moisture and to discard darkened pills because they have lost their potency.

Advise patient to change position slowly to minimize orthostatic hypotension.

Caution male patient about risk of priapism (persistent, painful erection), and urge him to seek medical help immediately if it occurs.

Category

Chemical class: Fluoroquinolone
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To reduce incidence or progression of inhalation anthrax after exposure to aerosolized Bacillus anthracis ,
IV:, Adults and children weighing more than 50 kg (110 lb). 500 mg (over 60 min for I.V. infusion) daily for 60 days. Children weighing less than 50 kg. 8 mg/kg (over 60 min for I.V. infusion) every 12 hr for 60 days. Maximum: 250 mg/dose. To treat acute maxillary sinusitis caused by Haemophilus influenzae, Moraxella catarrhalis, or Streptococcus pneumoniae ,

IV

,
Adults. 500 mg daily (over 60 to 90 min for I.V. infusion) for 10 to 14 days. Or 759 mg daily for 5 days. To treat acute exacerbation of chronic bacterial bronchitis caused by H. influenzae, H. parainfluenzae, M. catarrhalis, S. pneumoniae, or Staphylococcus aureus ,

IV

,
Adults.500 mg daily (over 60 to 90 min for I.V. infusion) for 7 days. To treat community-acquired pneumonia caused by Chlamydia pneumoniae, H. influenzae, H. parainfluenzae, Klebsiella pneumoniae, Legionella pneumophila, M. catarrhalis, Mycoplasma pneumoniae, S. aureus, or S. pneumoniae ,

IV

,
Adults.500 mg daily (over 60 to 90 min for I.V. infusion) for 7 to 14 days. Alternatively, for infection caused by C. pneumoniae, H. influenzae, H. parainfluenzae, M. pneumoniae, or S. pneumoniae, 750 mg daily (over 60 to 90 min for I.V. infusion) for 5 days. To treat uncomplicated UTI caused by Escherichia coli, K. pneumoniae, or Staphylococcus saprophyticus levofloxacin 582 ,

IV

,
Adults. 250 mg daily (over 60 to 90 min for I.V. infusion) for 3 days. To treat complicated UTI caused by Enterococcus faecalis, E. cloacae, E. coli, K. pneumoniae, Proteus mirabilis, or Pseudomonas aeruginosa or acute pyelonephritis caused by E. coli ,

IV

,
Adults. 250 mg daily (over 60 to 90 min for I.V. infusion) for 10 days. To treat complicated UTI caused by E. coli, K. pneumoniae, or P. mirabilis or acute pyelonephritis caused by E. coli ,
IV:,
Adults. 750 mg daily (over 90 min for I.V. infusion) for 5 days. To treat mild to moderate skin and softtissue infections caused by S. aureus or Streptococcus pyogenes ,

IV

,
Adults. 500 mg daily (over 60 to 90 min for I.V. infusion) for 7 to 10 days. To treat complicated skin and soft-tissue infections caused by methicillin-sensitive Enterococcus faecalis, Proteus mirabilis, S. aureus, or S. pyogenes; to treat nosocomial pneumonia caused by S. aureus, Pseudomonas aeruginosa, Serratia marcescens, E. coli, K. pneumoniae, H. influenzae, or S. pneumoniae ,

IV

,
Adults.750 mg daily (over 60 to 90 min for I.V. infusion) for 7 to 14 days. To treat chronic bacterial prostatitis caused by E. coli, E. faecalis, or S. epidermidis ,

IV

,
Adults. 500 mg daily (over 60 to 90 min for I.V. infusion) for 28 days.
DOSAGE ADJUSTMENT For complicated UTI in patients with creatinine clearance of 10 to 19 ml/min/1.73 m2, 250 mg initially and then maintenance dosage of 250 mg every 48 hr. For complicated skin and softtissue infections and nosocomial pneumonia when creatinine clearance is 19 ml/ min/1.73 m2or less, 750 mg initially and then maintenance dosage of 500 mg every 48 hr; when creatinine clearance is 20 to 49 ml/min/1.73 m2, 750 mg initially and then maintenance dosage of 750 mg every 48 hr. For all other indications, when creatinine clearance is 19 ml/min/1.73 m2or less, 500 mg initially and then maintenance of 250 mg every 48 hr; when creatinine clearance is 20 to 49 ml/min/1.73 m2, 500 mg initially and then maintenance dosage of 250 mg every 24 hr.

Mechanism of Action

Interferes with bacterial cell replication by inhibiting the bacterial enzyme DNA gyrase, which is essential for replication and repair of bacterial DNA.

Contraindications

Hypersensitivity to levofloxacin, other fluoroquinolones, or their components

Interactions

aluminum-, calcium-, or magnesium-containing antacids; didanosine; iron; sucralfate; zinc: Reduced GI absorption of levofloxacin antineoplastics: Decreased blood levofloxacin level
cimetidine: Increased blood levofloxacin level cyclosporine: Increased risk of nephrotoxicity
NSAIDs: Possibly increased CNS stimulation and risk of seizures oral anticoagulants: Increased anticoagulant effect and risk of bleeding oral antidiabetic : Possibly hyperglycemia or hypoglycemia
theophylline: Increased blood theophylline level and risk of toxicity sun exposure: Increased risk of photosensitivity

Side Efect

CNS: Anxiety, CNS stimulation, dizziness, fever, headache, increased ICP, insomnia, light-headedness, nervousness, paranoia, peripheral neuropathy, psychosis, seizures, sleep disturbance, suicidal ideation
CV: Arrhythmias, leukocytoclastic vasculitis, prolonged QT interval, torsades de pointes, vasculitis, vasodilation
EENT: Blurred vision, decreased visual acuity, diplopia, dysphonia, scotoma, taste perversion, tinnitus
ENDO: Hyperglycemia, hypoglycemia
GI: Abdominal pain, acute hepatic necrosis or failure, anorexia, constipation, diarrhea, flatulence, hepatitis, hepatotoxicity, indigestion, jaundice, nausea, pseudomembranous levofloxacin 583 J K L colitis, vomiting
GU: Acute renal failure or insufficiency, crystalluria, interstitial nephritis, vaginal candidiasis
HEME: Agranulocytosis, aplastic anemia, eosinophilia, hemolytic anemia, leukopenia, pancytopenia, thrombocytopenia
MS: Arthralgia, back pain, myalgia, rhabdomyolysis, tendon or muscle rupture
RESP: Allergic pneumonitis
SKIN: Photosensitivity, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, multiorgan failure, serum sickness

Cautions

Use levofloxacin cautiously in patients with renal insufficiency. Monitor renal function as appropriate during treatment.

Use drug cautiously in patients with CNS disorders, such as epilepsy, that may lower the seizure threshold. Also use cautiously in patients taking corticosteroids, especially elderly patients, because of increased risk of tendon rupture.

Expect to obtain culture and sensitivity tests before levofloxacin treatment begins.

Avoid giving drug within 2 hours of antacids.

Give parenteral form over 60 to 90 minutes, depending on dosage, because bolus or rapid I.V. delivery may cause hypotension.
WARNING Stop levofloxacin at first sign of hypersensitivity, including rash and jaundice, because drug may lead to anaphylaxis. Reaction may occur after first dose. Expect to give epinephrine and provide supportive care.

Monitor blood glucose level, especially in diabetic patient who takes an oral antidiabetic or uses insulin, because levofloxacin may alter blood glucose level. If so, notify prescriber, stop drug immediately if patient has hypoglycemia, and provide prescribed treatment.

Monitor QT interval if needed. If it lengthens, notify prescriber at once and stop drug. Patients with hypokalemia, significant bradycardia, or cardiomyopathy and those receiving a class IA or III antiarrhythmic shouldn’t receive levofloxacin.

Notify prescriber if patient has symptoms of peripheral neuropathy (pain; burning; tingling; numbness; weakness; altered sensations of light touch, pain, temperature, position sense, or vibration sense), which could be permanent; or CNS abnormalities (seizures, psychosis, increased ICP or CNS stimulation), which may lead to more serious

Side Efect

, such as suicidal ideation. In each case, expect to discontinue levofloxacin.

Watch for evidence of tendon rupture (inflammation, pain, swelling) during and up to several months after therapy, especially in children, elderly patients, patients receiving corticosteroids, and patients with kidney, heart, and lung transplants. Notify prescriber about suspected tendon rupture, and have patient rest and refrain from exercise until tendon rupture has been ruled out. If present, expect to provide supportive care, as ordered.

Monitor patient’s bowel elimination. If diarrhea develops, obtain stool culture to check for pseudomembranous colitis. If confirmed, expect to stop drug and give fluid, electrolytes, and antibiotics effective against Clostridium difficile.

PATIENT SAFTY

If patient will take oral solution form of levofloxacin, tell him to take it 1 hour before or 2 hours after eating.

Advise patient to increase fluid intake during therapy to prevent crystalluria.

Direct patient to take an antacid, didanosine, iron, sucralfate, or zinc at least 2 hours before or after levofloxacin.

Tell patient to complete the drug as prescribed, even if symptoms subside.

Urge patient to avoid excessive sun exposure and to wear sunscreen because of increased risk of photosensitivity. Tell patient to notify prescriber at first sign.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Tell patient to stop drug and notify prescriber if he develops tendon pain or inflammation or abnormal changes in motor or sensory function.

Urge patient to stop drug and tell prescriber about rash or other allergic reaction.

Advise diabetic patient to monitor blood glucose level and reportchanges.

Urge patient to tell prescriber about severe levofloxacin 584 diarrhea, even if it’s more than 2 months after drug therapy ends. Additional treatment may be needed.

Advise patient to notify prescriber about heart palpitations or loss of consciousness. An ECG may be needed to detect adverse drug effects on the patient’s heart.

Category

Chemical class: Morphinan derivative
Therapeutic class: Analgesic, anesthesia adjunct

Pregnancy category: Not rated

Controlled substance schedule: II

Indications

To relieve moderate to severe pain
Adults.2 mg every 6 to 8 hr, p.r.n. Increased to 3 mg every 6 to 8 hr, if indicated.
I.V.INJECTION
Adults.Up to 1 mg every 3 to 6 hr, p.r.n. Maximum: 8 mg daily for non–opioiddependent patients. I.M.OR SUBCUTANEOUS INJECTION
Adults. 1 to 2 mg every 6 to 8 hr, p.r.n. Maximum: 8 mg daily for non–opioiddependent patients. To provide preoperative sedation I.M.OR SUBCUTANEOUS INJECTION
Adults. 1 to 2 mg 60 to 90 min before procedure. Route Onset Peak Duration P.O. 10–60 min 90–120 min 4–5 hr I.V. Unknown In 20 min 4–5 hr I.M. Unknown 60 min 4–5 hr SubQ Unknown 60–90 min 4–5 hr

Mechanism of Action

Decreases intracellular level of cyclic adenosine monophosphate by inhibiting adenylate cyclase, which regulates release of pain neurotransmitters, such as substance P, gamma-aminobutyric acid, dopamine, acetylcholine, and noradrenaline. Levorphanol also stimulates mu and kappa opioid receptors, altering perception of and emotional response to pain.

Incompatibilities

Don’t mix levorphanol tartrate with solutions that contain aminophylline, ammonium chloride, amobarbital sodium, chlorothiazide sodium, heparin sodium, methicillin sodium, nitrofurantoin sodium, novobiacin sodium, pentobarbital sodium, perphenazine, phenobarbital sodium, phenytoin, secobarbital sodium, sodium bicarbonate, sodium iodide, sulfadiazine sodium, sulfisoxazole diethanolamine, or thiopental sodium.

Contraindications

Acute alcoholism, acute or severe asthma, anoxia, hypersensitivity to levorphanol tartrate or its components, increased intracranial pressure, respiratory depression, upper airway obstruction

Interactions

alfentanil, CNS depressants, fentanyl, sufentanil: Possibly increased CNS and respiratory depression and hypotension anticholinergics: Increased risk of severe constipation antidiarrheals, such as difenoxin and atropine, kaolin, and loperamide: Increased risk of severe constipation and increased CNS depression antihypertensives: Increased risk of hypotension buprenorphine: Possibly decreased therapeutic effects of levorphanol and increased risk of respiratory depression hydroxyzine: Increased risk of CNS depression and hypotension metoclopramide: Possibly antagonized effects of metoclopramide naloxone,
naltrexone: Decreased therapeutic effects of levorphanol neuromuscular blockers: Increased risk of prolonged CNS and respiratory depression
alcohol use: Possibly increased CNS and respiratory depression and hypotension

Side Efect

CNS: Amnesia, coma, confusion, delusions, depression, dizziness, drowsiness, dyskinesia, hypokinesia, insomnia, nervousness, personality disorder, seizures
CV: Bradycardia, cardiac arrest, hypotension, orthostatic hypotension, palpitations, shock, tachycardia levorphanol tartrate 585 J K L
EENT: Abnormal vision, diplopia, dry mouth
GI: Abdominal pain, biliary tract spasm, constipation, hepatic failure, indigestion, nausea, vomiting
GU: Dysuria, urine retention
RESP: Apnea, hyperventilation
SKIN: Cyanosis, pruritus, rash, urticaria
Other: Injection site pain, redness, and swelling; physical and psychological dependence

Cautions

WARNING Be aware that levorphanol may be habit-forming.

Give drug with food if GI distress occurs.

If respiratory depression occurs, expect to administer naloxone to reverse it.

Monitor supine and standing blood pressure, and notify prescriber of orthostatic hypotension.

Carefully assess for

Side Efect

in elderly patients; they are especially sensitive to drug and are at increased risk for constipation.

PATIENT SAFTY

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to avoid alcoholic beverages while taking levorphanol.

Direct patient to change position slowly to minimize orthostatic hypotension.

Advise patient to notify prescriber if constipation, nausea, or vomiting occurs.

If patient reports dry mouth, suggest that she use sugarless candy or gum or ice chips.

Category

Chemical class: Synthetic thyroxine (T4)
Therapeutic class: Thyroid hormone replacement Pregnancy category: A

Indications

To treat mild hypothyroidism
Adults.Initial: 50 mcg daily, increased by 25 to 50 mcg every 2 to 3 wk until desired response occurs or therapeutic blood level is reached. Maintenance: 75 to 125 mcg daily.
DOSAGE ADJUSTMENT For elderly patients and those with cardiovascular disease or chronic hypothyroidism, initial dosage usually reduced to 12.5 to 25 mcg daily and then increased by 12.5 to 25 mcg every 3 to 4 wk until desired response occurs. For elderly patients, maintenance dosage is limited to 75 mcg daily. Children over age 10. 2 to 3 mcg/kg daily. Usual: 150 to 200 mcg daily. Children ages 6 to 10. 4 to 5 mcg/kg daily. Usual: 100 to 150 mcg daily. Children ages 1 to 5. 3 to 5 mcg/kg daily. Usual: 75 to 100 mcg daily. Infants ages 6 to 12 months. 5 to 6 mcg/kg daily. Usual: 50 to 75 mcg daily. Infants under age 6 months. 5 to 6 mcg/kg daily. Usual: 25 to 50 mcg daily. To treat severe hypothyroidism
Adults. Initial: 12.5 to 25 mcg daily. Increased by 25 mcg every 2 to 3 wk until desired response occurs or therapeutic blood level is reached. Maintenance: 75 to 125 mcg daily. Maximum: 200 mcg daily. Children over age 10. 2 to 3 mcg/kg daily. Usual: 150 to 200 mcg daily. Children ages 6 to 10. 4 to 5 mcg/kg daily. Usual: 100 to 150 mcg daily. Children ages 1 to 5. 3 to 5 mcg/kg daily. Usual: 75 to 100 mcg daily. Infants ages 6 to 12 months. 5 to 6 mcg/kg daily. Usual: 50 to 75 mcg daily. Infants under age 6 months. 5 to 6 mcg/kg daily. Usual: 25 to 50 mcg daily. I.V.OR
I.M.INJECTION
Adults. 50 to 100 mcg daily until therapeutic blood level is reached. Children.75% of usual P.O. dose daily until therapeutic blood level is reached. To treat myxedema coma
I.V.INJECTION
Adults. 200 to 500 mcg on day 1. If no significant improvement, 100 to 300 mcg on day 2. Daily dose continued as prescribed until therapeutic blood level is reached and levothyroxine sodium 586 P.O. administration is tolerated. Children.75% of usual P.O. dose daily until therapeutic blood level is reached and P.O. administration is tolerated. Route Onset Peak Duration P.O. 3–5 days 3–4 wk 1–3 wk I.V. 6–8 hr 24 hr Unknown I.M. Unknown Unknown 1–3 wk

Mechanism of Action

Replaces endogenous thyroid hormone, which may exert its physiologic effects by controlling DNA transcription and protein synthesis. Levothyroxine has all the following actions of endogenous thyroid hormone. The drug:

increases energy expenditure

accelerates the rate of cellular oxidation, which stimulates body tissue growth, maturation, and metabolism

regulates differentiation and proliferation of stem cells

aids in myelination of nerves and development of synaptic processes in the nervous system

regulates growth

decreases blood and hepatic cholesterol concentrations

enhances carbohydrate and protein metabolism, increasing gluconeogenesis and protein synthesis.

Contraindications

Acute MI (unless caused or complicated by hyperthyroidism), hypersensitivity to levothyroxine or its components, uncorrected adrenal insufficiency, untreated thyrotoxicosis

Interactions

adrenocorticoids: Possibly adrenocorticoid
DOSAGE ADJUSTMENTs as thyroid status changes aluminumand magnesium-containing antacids, bile acid sequestrants, calcium carbonate, cation exchange resins, cholestyramine, colestipol, ferrous sulfate, kayexalate, orlistat, sucralfate: Possibly reduced effects of levothyroxine amiodarone, iodide: Possibly hyperthyroidism
beta blockers: Possibly impaired action of beta blockers and decreased conversion of T4to triiodothyronine (T3) cholestyramine, colestipol: Delayed or inhibited levothyroxine absorption digoxin: Reduced digoxin effects estrogen, phenylbutazone,
phenytoin: Reduced binding of levothyroxine to protein, possibly requiring increased levothyroxine dosage insulin, oral antidiabetic : Possibly uncontrolled diabetes mellitus, requiring increased dosage of insulin or oral antidiabetic drug ketamine: Possibly hypertension and tachycardia maprotiline: Increased risk of arrhythmias oral anticoagulants: Altered anticoagulant activity, possibly need for anticoagulant
DOSAGE ADJUSTMENT selective serotonin reuptake inhibitors, tricyclic and tetracyclic antidepressants: Increased therapeutic and toxic effects of both sympathomimetics: Increased risk of coronary insufficiency in patients with coronary artery disease
theophylline: Decreased theophylline clearance dietary fiber, soybean flour (infant formula), walnuts: Possibly decreased absorption of levothyroxine from GI tract

Side Efect

CNS: Fatigue, headache, insomnia, somnolence
ENDO: Hyperthyroidism (with overdose)
GI: Dysphagia
MS: Muscle weakness, myalgia, slipped capital femoral epiphysis
SKIN: Alopecia (transient), rash, urticaria
Other: Weight gain

Cautions

Administer levothyroxine tablets as a single daily dose 30 to 60 minutes before breakfast. If patient has difficulty swallowing, crush tablet and suspend in a small amount of water or food.

To prevent decreased drug absorption, give oral levothyroxine at least 4 hours before or after aluminumor magnesiumcontaining antacids, bile acid sequestrants, calcium carbonate, cation exchange resins, cholestyramine, colestipol, ferrous sulfate, levothyroxine sodium 587 J K L kayexalate, or sucralfate.

Expect to give drug I.V. or I.M. if patient can’t take tablets. Be aware that drug shouldn’t be given subcutaneously.

For I.V. use, reconstitute drug by adding 5 ml of normal saline solution.

Monitor PT of patient who is receiving anticoagulants; she may require a dosage adjustment.

Monitor blood glucose level of diabetic patient. Prescriber may reduce antidiabetic drug dosage as thyroid hormone level enters therapeutic range.

Expect patient to undergo thyroid function tests regularly during levothyroxine therapy.

PATIENT SAFTY

Inform patient that levothyroxine replaces a hormone that is normally produced by the thyroid gland and that she’ll probably need to take drug for life.

Instruct patient to take drug at least 30 minutes before breakfast because drug absorption is increased on an empty stomach and evening doses may cause insomnia.

Stress the need to take levothyroxine with a full glass of water to avoid choking, gagging, having tablet stick in throat, and developing heartburn afterward.

Instruct patient to separate iron and calcium supplements and antacids by at least 4 hours from levothyroxine doses.

Inform patient that drug may require a few weeks to take effect.

Advise patient not to stop drug or change dosage unless instructed by prescriber.

Instruct patient to report signs of hyperthyroidism, such as diarrhea, excessive sweating, heat intolerance, insomnia, palpitations, weight loss, chest pain, shortness of breath, leg cramps, headache, nervousness, irritability, tremors, changes in appetite, vomiting, fever, and changes in menstrual periods.

Tell patient to notify prescriber if rash or hives develop during drug use.

Inform patient that transient hair loss may occur during first few months of levothyroxine therapy.

Instruct female patient of childbearing age to notify prescriber immediately if she becomes pregnant because levothyroxine dosage may need to be increased.

Category

Chemical class: Aminoacetamide
Therapeutic class: Class IB antiarrhythmic, local anesthetic

Pregnancy category: B

Indications

To treat ventricular tachycardia or ventricular fibrillation
IV: AND INJECTION
Adults.Loading: 50 to 100 mg (or 1 to 1.5 mg/kg), given at 25 to 50 mg/min. If desired response isn’t achieved after 5 to 10 min, second dose of 25 to 50 mg (or 0.5 to 0.75 mg/kg) given every 5 to 10 min until maximum loading dose (300 mg in 1 hr) has been given. Maintenance: 20 to 50 mcg/kg/min (1 to 4 mg/min) by continuous infusion. Smaller bolus dose repeated 15 to 20 min after start of infusion if needed to maintain therapeutic blood level. Maximum: 300 mg (or 3 mg/kg) over 1 hr. Children.Loading: 1 mg/kg. Maintenance: 30 mcg/kg/min by continuous infusion. Maximum: 3 mg/kg.
DOSAGE ADJUSTMENT For elderly patients receiving I.V. lidocaine to treat arrhythmias and for patients with acute hepatitis or decompensated cirrhosis, loading dose and continuous infusion rate reduced by 50%.
I.M.INJECTION
Adults.300 mg, repeated after 60 to 90 min, if needed. To provide topical anesthesia for skin or mucous membranes FILM-FORMING GEL, JELLY, OR OINTMENT
Adults. Thin layer applied to skin or mucous membranes as needed before procedure. TRANSDERMAL PATCH
Adults. 1 to 3 patches applied over most painful area only once for up to 12 hr withlidocaine hydrochloride 588 in a 24-hr period. To provide topical anesthesia before venous access procedures POWDER Children ages 3 to 18. Compressed gas application of powder to selected skin site 1 to 3 minutes before procedure. Route Onset Peak Duration I.V. 45–90 sec Immediate 10–20 min I.M. 5–15 min Unknown 60–90 min Topical 2–5 min Unknown 0.5–1 hr

Mechanism of Action

Combines with fast sodium channels in myocardial cell membranes, which inhibits sodium influx into cells and decreases ventricular depolarization, automaticity, and excitability during diastole. Lidocaine also blocks nerve impulses by decreasing the permeability of neuronal membranes to sodium, which produces local anesthesia.

Contraindications

Adams-Stokes syndrome; hypersensitivity to lidocaine, amide anesthetics, or their components; severe heart block (without artificial pacemaker); Wolff-ParkinsonWhite syndrome

Interactions

beta blockers,
cimetidine: Increased blood lidocaine level and risk of toxicity MAO inhibitors, tricyclic antidepressants: Risk of severe, prolonged hypertension mexiletine, tocainide: Additive cardiac effects neuromuscular blockers: Possibly increased neuromuscular blockade phenytoin, procainamide: Increased cardiac depression

Side Efect

CNS: Anxiety, confusion, difficulty speaking, dizziness, hallucinations, lethargy, paresthesia, seizures
CV: Bradycardia, cardiac arrest, hypotension, new or worsening arrhythmias
EENT: Blurred vision, diplopia, tinnitus
GI: Nausea
MS: Muscle weakness, myalgia
RESP: Respiratory arrest or depression
Other: Hypersensitivity; injection site burning, irritation, petechiae, redness, stinging, swelling, and tenderness; worsened pain

Cautions

Observe for respiratory depression after bolus injection and during I.V. infusion of lidocaine.

Keep life-support equipment and vasopressors nearby during I.V. use in case of respiratory depression or other reactions.

Carefully check prefilled syringes before using. Use only syringes labeled “for cardiac arrhythmias”for I.V. administration.

As ordered, titrate I.V. dose to minimum amount needed to prevent arrhythmias.

During I.V. administration, place patient on cardiac monitor, as ordered, and closely observe her at all times. Monitor for worsening arrhythmias, widening QRS complex, and prolonged PR interval—possible signs of drug toxicity.

Check blood drug level, as ordered. Therapeutic level is 2 to 5 mcg/ml.

If signs of toxicity, such as dizziness, occur, notify prescriber and expect to discontinue or slow infusion.

Give I.M. injection in deltoid muscle only.

Apply lidocaine jelly or ointment to gauze or bandage before applying to skin.

Monitor vital signs as well as BUN and serum creatinine and electrolyte levels during and after therapy.

PATIENT SAFTY

Inform patient who receives lidocaine as an anesthetic that she’ll feel numbness.

Advise patient to report difficulty speaking, dizziness, injection site pain, nausea, numbness or tingling, and vision changes.

Caution patient to keep lidocaine topical preparations and patches out of reach of children and pets.

Tell patient to wash hands thoroughly after handling lidocaine topical forms or patch and to avoid getting drug in eyes.

If patient uses patches, tell her to store them in their sealed envelopes until needed and to apply immediately after removing from the envelope. Tell patient to remove patch if irritation or burning occurs at the site and not to reapply until irritation is gone.

Tell patient to fold used patches so that the adhesive side sticks to itself and discard where children or pets cannot get to them.

Category

Chemical class: Lincosamide
Therapeutic class: Bacteriostatic or bactericidal antibiotic

Pregnancy category: C

Indications

To treat serious respiratory, skin, and soft-tissue infections caused by susceptible strains of streptococci, pneumococci, and staphylococci Adults and adolescents.500 mg every 6 to 8 hr. Children over age 1 month. 7.5 to 15 mg/ kg every 6 hr; or, 10 to 20 mg/kg every 8 hr.
IV:
Adults. 600 mg to 1 g every 8 to 12 hr. Maximum: 8 g daily in divided doses for life-threatening infection. Children over age 1 month.10 to 20 mg/ kg/day in divided doses every 8 to 12 hr, depending on severity of infection.
I.M.INJECTION Adults and adolescents.600 mg every 12 to 24 hr. Children over age 1 month. 10 mg/kg every 12 to 24 hr.
DOSAGE ADJUSTMENT Dosage reduced by 25% to 30% for patients with severely impaired renal function.

Mechanism of Action

Inhibits protein synthesis in susceptible bacteria by binding to 50S subunit of bacterial ribosomes and preventing peptide bond formation, causing bacterial cells to die.

Incompatibilities

Don’t give lincomycin with novobiocin or kanamycin.

Contraindications

Hypersensitivity to lincomycin, clindamycin, or their components

Interactions

antimyasthenic : Possibly antagonized effects of these chloramphenicol, clindamycin, erythromycin: Possibly blocked access of lincomycin to its site of action hydrocarbon inhalation anesthetics, neuromuscular blockers: Increased neuromuscular blockade, possibly severe respiratory depression opioid analgesics: Increased risk of prolonged or increased respiratory depression

Side Efect

CNS: Fever, vertigo
CV: Cardiac arrest and hypotension (with rapid administration)
EENT: Glossitis, stomatitis, tinnitus
GI: Abdominal cramps, colitis, diarrhea, nausea, pseudomembranous colitis, rectal candidiasis, vomiting
GU: Vaginal candidiasis
HEME: Agranulocytosis, eosinophilia, leukopenia, neutropenia, thrombocytopenic purpura
SKIN: Erythema multiforme, rash, StevensJohnson syndrome, urticaria
Other: Anaphylaxis, angioedema, superinfection

Cautions

Expect to obtain a specimen for culture and sensitivity testing before giving first dose of lincomycin.
WARNING Be aware that some lincomycin preparations contain benzyl alcohol, which can cause a fatal toxic syndrome in neonates or premature infants characterized by CNS, respiratory, circulatory, and renal impairment and metabolic acidosis. Because drug enters breast milk, breastfeeding patient may need to stop drug or stop breast-feeding.

Dilute 600-mg dose in at least 100 ml D5W, D10W, normal saline solution, dextrose 5% in normal saline solution, or other compatible diluent recommended by manufacturer. Dilute higher doses in 100 ml of a compatible diluent for each gram being given—for example, dilute a 3-g dose in at least 300 ml of diluent. Use diluted solution within 24 hours if stored at room temperature.
WARNING Give lincomycin over at least 1 hour for each gram being administered. For example, infuse 1 g over 1 hour and 3 g over 3 hours. Too-rapid infusion may result in cardiac arrest or hypotension. lincomycin hydrochloride 590
WARNING Monitor patient for hypersensitivity reaction, such as rash, pruritus, wheezing, and dysphagia from laryngeal edema. If a reaction occurs, stop infusion and notify prescriber immediately. If anaphylaxis occurs, give epinephrine, antihistamines, oxygen, and corticosteroids, as prescribed. Be aware that patients with a history of asthma or significant allergies are at increased risk of hypersensitivity.

Observe patient for evidence of superinfection, such as vaginal itching and sore mouth.

Monitor patient for signs of pseudomembranous colitis, such as watery, loose stools. Patients with a history of GI disease, particularly colitis or regional enteritis, are at increased risk for colitis. In elderly patients, antibiotic-related diarrhea may be more severe and less well tolerated. Notify prescriber if severe or prolonged diarrhea develops; it may indicate pseudomembranous colitis caused by Clostridium difficile. Expect to withhold lincomycin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Monitor results of liver and renal function tests, CBC, and platelet counts periodically during lincomycin therapy.

Before diluting drug, store it at a controlled room temperature of 68° to 77° F (20° to 25° C).

PATIENT SAFTY

Advise patient to take lincomycin capsules with a full glass of water on an empty stomach 1 hour before or 2 hours after meals to maximize drug’s effectiveness.

Review with patient possibly serious

Side Efect

, such as difficulty breathing, rash, and chest tightness, and tell her to report any that occur.

Inform patient that yogurt or buttermilk can help maintain intestinal flora and may decrease the risk of diarrhea.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and can be serious, requiring prompt treatment.

Stress the importance of following dosage regimen and keeping follow-up medical and laboratory appointments.

Category

Chemical class: Benzene derivative
Therapeutic class: Pediculicide, scabicide

Pregnancy category: B

Indications

To treat scabies and pediculosis CREAM, LOTION Adults and children.For scabies, thin layer applied once over entire skin surface. For pediculosis, thin layer applied once to affected skin and hair. SHAMPOO Adults and children. 30 ml (for short hair) or 45 ml (for long hair) applied to dry hair and worked into lather for 4 to 5 min.

Mechanism of Action

Penetrates parasite skeleton and inhibits neuronal membrane function, causing seizures and death. Lindane also kills parasite eggs.

Contraindications

Hypersensitivity to lindane or its components, prematurity (in neonates), seizure disorders

Interactions

use of oil-based hair products: Possibly increased absorption of lindane

Side Efect

CNS: Dizziness, irritability, nervousness, restlessness, seizures, unsteadiness
SKIN: Erythema, pruritus, rash, urticaria

Cautions

Use lindane cautiously in patients at risk for CNS toxicity, such as infants, elderly patients, and patients weighing less than 110 lb (50 kg).

Wear gloves when applying drug. If another person will apply drug, supply gloves for use.

For scabies, apply thin layer of preparation to dry skin and rub in thoroughly. Trim patient’s nails, and apply under nails with toothbrush. Apply to body from neck down, including soles. Leave drug on for 8 to 12 hours (usually overnight), and then remove with bath or shower.

Expect to reduce application time for infants and children to 6 to 8 hours, as prescribed, because of risk of systemic absorption.

Keep lindane away from mouth and eyes. Don’t use on open wounds, cuts, or sores.

Expect to give topical steroids or oral antihistamines to reduce pruritus, which may continue for several weeks with scabies.

For hospitalized patients, use special linen-handling precautions until treatment is completed.
WARNING Be aware that lindane may cause seizures or other adverse CNS reactions. Use it only after other treatments have been tried.

Monitor immunocompromised patients closely because they’re at increased risk for

Side Efect

.

PATIENT SAFTY

Inform patient that lindane is for onetime use but may be reapplied after 1 week if she finds live lice or nits (eggs).

Caution patient to avoid eyes, mucous membranes, and open areas of skin when applying drug and not to inhale vapors.

Instruct patient (or parents of a child) to wear gloves when applying drug.

For scabies, instruct patient to shake lotion bottle well before using and to apply lotion or cream in a thin layer all over body from neck down, avoiding face and scalp. Direct her to leave drug on for 8 to 12 hours and then wash it off in the bath or shower. Explain that itching may persist for several weeks after treatment.

For pubic lice, instruct patient to shake lotion bottle well before using and to apply a thin layer of lotion to pubic hair and skin as well as to groin, thighs, and lower stomach if they’re also affected. Direct her to leave lotion on for 12 hours and then thoroughly wash it off in the bath or shower.

For head lice, instruct patient to shake lotion bottle well before using and to apply lotion to affected areas of head and scalp as well as nearby hairy areas and rub it in well. Tell her to leave lotion on for 12 hours and then thoroughly wash it off.

For head or pubic lice, instruct patient to wash and dry her hair before applying lindane shampoo, especially if she uses oilbased hair products. Instruct her to shake bottle well before using and then apply shampoo to dry hair, working it in thoroughly and adding a small amount of water if needed to form good lather. Direct her to wait 4 minutes, rinse her hair well, and then dry it with a clean towel. Instruct her to use a fine-toothed comb or tweezers to remove nits or nit shells. Direct patient not to use shampoo again for 7 days and then only if she finds live lice. Caution patient not to use shampoo in the shower to avoid getting it in her eyes and mouth.

Advise patient to wash lindane off her skin and to contact prescriber if irritation (severe itching, hives, or redness) occurs.

Explain that if lice come back, the problem is probably reinfestation rather than treatment failure.

Advise patient to notify family members and sexual contacts about infestation.

Category

Chemical class: Oxazolidinone
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To treat vancomycin-resistant Enterococcus faecium infections, including bacteremia ORAL SUSPENSION, ,

IV

Adults and adolescents. 600 mg every 12 hr for 14 to 28 days. Infants and children.10 mg/kg every 8 hr for 14 to 28 days. To treat nosocomial pneumonia caused by Staphylococcus aureus (methicillinsusceptible and -resistant strains) or Streptococcus pneumoniae (penicillinsusceptible strains only) and communityacquired pneumonia, including accompanying bacteremia, caused by S. aureus (methicillin-susceptible strains only) or S. pneumoniae (penicillin-susceptible strains only); to treat complicated skin linezolid 592 and soft-tissue infections, including diabetic foot infections without concomitant osteomyelitis, caused by S. aureus (methicillin-susceptible and -resistant strains), Streptococcus pyogenes, or Streptococcus agalactiae ORAL SUSPENSION, ,

IV

Adults and adolescents.600 mg every 12 hr for 10 to 14 days. Infants and children. 10 mg/kg every 8 hr for 10 to 14 days. To treat uncomplicated skin and softtissue infections caused by S. aureus (methicillin-susceptible strains only) or S. pyogenes ORAL SUSPENSION,
Adults. 400 mg every 12 hr for 10 to 14 days. Adolescents. 600 mg every 12 hr for 10 to 14 days. Children age 5 to 11. 10 mg/kg every 12 hr for 10 to 14 days. Infants and children to age 5. 10 mg/kg every 8 hr.

Incompatibilities

Don’t add other to linezolid solution. Don’t infuse linezolid in same I.V. line as amphotericin B, chlorpromazine hydrochloride, co-trimoxazole, diazepam, erythromycin lactobionate, pentamidine isethionate, or phenytoin sodium because these are physically incompatible. Don’t infuse linezolid with ceftriaxone sodium because these are chemically incompatible.

Contraindications

Carcinoid syndrome; concurrent therapy Polypeptide chain 70S initiation complex Amino acid Nonfunctioning 70S initiation complex Linezolid tRNA Messenger RNA 30S subunit 50S subunit 23S rRNA Polypeptide chain 70S initiation complex Amino acid Nonfunctioning 70S initiation complex Linezolid tRNA Messenger RNA 30S subunit 50S subunit 23S rRNA

Mechanism of Action

Linezolid inhibits bacterial protein synthesis by interfering with translation of ribonucleic acid (RNA) to protein. In bacteria, protein synthesis begins with binding of a 30S ribosomal subunit and a 50S ribosomal subunit to a messenger RNA (mRNA) molecule to form a 70S initiation complex. The 50S ribosomal subunit consists of 23S ribosomal RNA (rRNA) and other ribosomal subunits. Then translation begins. Transfer RNA (tRNA) attaches to the 50S subunit and brings specific amino acids into place. As the tRNA and amino acids fall into place, they are joined together by peptide bonds and elongate to form a polypeptide chain, as shown below left. This chain eventually combines with other polypeptide chains to form a complete protein molecule. After translation is complete, the ribosomal subunits fall away and are ready to combine with more mRNA to start the translation process over again. Linezolid binds to a site on the bacterial 23S rRNA of the 50S subunit. This action prevents formation of a functional 70S initiation complex, an essential component of the bacterial translation. Without proper protein production, as shown below right, susceptible bacteria are unable to multiply. Linezolid is bacteriostatic against staphylococci and enterococci and bactericidal against most streptococci. with buspirone, dopaminergic agents, meperidine, sympathomimetic agents, serotonin 5-HT1receptor agonists, serotonin reuptake inhibitors, tricyclic antidepressants, or vasopressive agents without careful monitoring; hypersensitivity to linezolid or its components; phenylketonuria; thyrotoxicosis; uncontrolled hypertension; use within 14 days of an MAO inhibitor

Interactions

adrenergics, including pseudoephedrine and phenylpropanolamine: Possibly increased blood pressure buspirone, meperidine, serotonergics, tricyclic antidepressants: Possibly serotonin syndrome carbamazepine, phenytoin, phenobarbital,
rifampin: Possibly decreased plasma linezolid level
MAO inhibitors: Increased risk of lifethreatening adverse effects tyramine-containing and beverages: Possibly hypertension

Side Efect

CNS: Dizziness, fever, headache, insomnia, optic and peripheral neuropathy, serotonin syndrome
CV: Hypertension
EENT: Oral candidiasis, tooth or tongue discoloration
GI: Abdominal pain, constipation, diarrhea, indigestion, nausea, pseudomembranous colitis, vomiting
GU: Vaginal candidiasis
HEME: Anemia, leukopenia, pancytopenia, thrombocytopenia
SKIN: Pruritus, rash
Other: Lactic acidosis

Cautions

Obtain body tissue and fluid specimens for culture and sensitivity tests, as ordered, before giving first dose of linezolid. Expect to start drug before test results are known.

Be aware that linezolid shouldn’t be used to treat catheter-related bloodstream infections, catheter-site infections, or infections caused by gram-negative bacteria because the risk of death is higher in these infections.

Infuse I.V. solution over 30 to 120 minutes with D5W, normal saline solution, or lactated Ringer’s solution.
WARNING Monitor CBC weekly, as ordered, to detect or track worsening myelosuppression in patients who need more than 2 weeks of therapy, who have preexisting myelosuppression and are receiving that produce bone marrow suppression, or who have chronic infection and are receiving or have received antibiotic therapy.

Notify prescriber if patient develops visual impairment that suggests optic neuropathy, such as changes in visual acuity or color vision, blurred vision, lost vision, or visual field defect. If optic or peripheral neuropathy develops, the drug may need to be stopped.

If patient takes a dopaminergic agent, sympathomimetic agent, or vasopressive agent, monitor blood pressure closely; if monitoring isn’t possible, linezolid shouldn’t be prescribed.

If patient takes buspirone, meperidine, a serotinergic, or a tricyclic antidepressant, watch closely for signs and symptoms of serotonin syndrome; if monitoring isn’t possible, linezolid shouldn’t be prescribed.

Assess bowel pattern daily. Also watch for secondary infection, including oral candidiasis and profuse, watery diarrhea.

PATIENT SAFTY

Caution patient with phenylketonuria that oral suspension contains phenylalanine.

Advise patient not to take OTC cold remedies without consulting prescriber because medications that contain pseudoephedrine or propanolamine may cause or worsen hypertension.

Instruct patient to avoid and beverages that contain large amounts of tyramine, including aged cheese, fermented or air-dried meats, sauerkraut, soy sauce, tap beers, red wines, and protein-rich that have been stored for long periods or poorly refrigerated.

Instruct patient to notify prescriber at once about severe diarrhea, even up to 2 months after linezolid therapy has ended, because additional treatment may be needed.

Also tell patient to report vision changes and changes in limb sensation (such as pins and needles, numbness, or tingling) because drug may need to be stopped. linezolid 594

Reassure patient with tooth discoloration that professional dental cleaning can restore tooth color.

Category

Chemical class: Synthetic triiodothyronine (T3)
Therapeutic class: Thyroid hormone replacement Pregnancy category: A

Indications

To treat mild hypothyroidism
Adults. Initial: 25 mcg daily. Increased by 12.5 to 25 mcg every 1 to 2 wk until response occurs. Maintenance: 25 to 50 mcg daily.
DOSAGE ADJUSTMENT For elderly patients and those with cardiovascular disease, initial dose reduced to 5 mcg daily and then increased by 5 mcg every 2 wk. To treat congenital hypothyroidism Adults and children.Initial: 5 mcg daily. Increased by 5 mcg every 3 to 4 days until desired response occurs. Maintenance: Highly individualized. To treat simple nontoxic goiter
Adults.Initial: 5 mcg daily. Increased by 5 to 10 mcg every 1 to 2 wk up to 25 mcg daily. Then increased by 12.5 to 25 mcg/wk, as indicated. Maintenance: 50 to 100 mcg daily. To treat myxedema
Adults. Initial: 2.5 to 5 mcg daily. Increased 5 to 10 mcg every 1 to 2 wk up to 25 mcg daily. Then increased by 12.5 to 25 mcg every 1 to 2 wk, as indicated. Maintenance: 25 to 50 mcg daily. To treat myxedema coma or premyxedema coma (severe hypothyroidism)
I.V.INJECTION
Adults. Initial: 25 to 50 mcg. Repeated every 4 to 12 hr according to patient’s response. Then P.O. therapy is resumed as soon as possible.
DOSAGE ADJUSTMENT When treating myxedema coma in patients with known or suspected cardiovascular disease, initial dose decreased to 10 to 20 mcg. To differentiate hyperthyroidism from euthyroidism (T3suppression test)
Adults.75 to 100 mcg daily for 7 days. Route Onset Peak Duration P.O. 24–72 hr 48–72 hr Up to 72 hr I.V. 2–4 hr 2 days Unknown

Mechanism of Action

Replaces endogenous thyroid hormone, which may exert its physiologic effects by controlling DNA transcription and protein synthesis. Like endogenous thyroid hormone, liothyronine:

increases energy expenditure

accelerates the rate of cellular oxidation, which stimulates body tissue growth, maturation, and metabolism

regulates differentiation and proliferation of stem cells

aids in myelination of nerves and development of synaptic processes in the nervous system

regulates growth

decreases blood and hepatic cholesterol concentrations

enhances carbohydrate and protein metabolism, increasing gluconeogenesis and protein synthesis.

Contraindications

Acute MI (unless caused or complicated by hypothyroidism), hypersensitivity to liothyronine or its components, uncorrected adrenal insufficiency, untreated thyrotoxicosis

Interactions

adrenocorticoids: Possibly need for adrenocorticoid
DOSAGE ADJUSTMENTs as thyroid status changes
beta blockers: Possibly impaired action of beta blockers cholestyramine, colestipol: Decreased liothyronine absorption digoxin: Reduced therapeutic effects of digoxin estrogen, phenylbutazone,
phenytoin: Reduced binding of liothyronine to protein, possibly requiring increased liothyronine dosage insulin, oral antidiabetic: Possibly uncontrolled diabetes mellitus, requiring increased dosage of insulin or oral antidiabetic ketamine: Possibly hypertension and tachycardia maprotiline: Increased risk of arrhythmias oral anticoagulants: Altered anticoagulant activity, possibly need for anticoagulant
DOSAGE ADJUSTMENT sympathomimetics: Increased risk of coronary insufficiency in patients with coronary artery disease
theophylline: Decreased theophylline clearance tricyclic antidepressants: Increased therapeutic and toxic effects of both

Side Efect

CNS: Insomnia
ENDO: Hyperthyroidism (with overdose)
SKIN: Alopecia (transient), rash, urticaria

Cautions

Be aware that liothyronine is used most often for rapid onset or rapidly reversible thyroid hormone replacement.

Administer tablet as a single daily dose before breakfast.

Give I.V. injections more than 4 hours but less than 12 hours apart.

Evaluate response to therapy by monitoring pulse rate and blood pressure.

Expect patient to undergo regular tests of thyroid function during therapy.

Monitor PT of patient receiving anticoagulants because she may require a dosage adjustment.

Frequently monitor blood glucose level of diabetic patient. Prescriber may reduce antidiabetic drug dosage as thyroid hormone level enters therapeutic range.

Be aware that liothyronine is used in T3 suppression test to differentiate hyperthyroidism from euthyroidism (normal thyroid function). For this test,131I uptake test is performed before and after liothyronine administration. Suppression of131I uptake by 50% indicates normal thyroid function.

PATIENT SAFTY

Inform patient that liothyronine usually is taken for life. Caution her not to discontinue drug or change dosage unless instructed by prescriber.

Instruct patient to take drug before breakfast; evening doses may cause insomnia.

Advise patient to report signs of hyperthyroidism, such as chest pain, excessive sweating, heat intolerance, increased pulse rate, nervousness, and palpitations.

Inform patient that transient hair loss may occur during first few months of therapy.

Instruct diabetic patient to monitor blood glucose level frequently because antidiabetic drug dosage may need to be reduced.

Inform patient of need for periodic blood tests to monitor drug effectiveness.

Category

Chemical class: Acylated human glucagonlike peptide-1
Therapeutic class: Antidiabetic

Pregnancy category: C

Indications

To improve glycemic control as an adjunct to diet and exercise in patients with type 2 diabetes mellitus SUBCUTANEOUS INJECTION
Adults.Initial: 0.6 mg daily for 1 wk., then increased to 1.2 mg daily. Maximum: 1.8 mg daily. Route Onset Peak Duration SubQ Unknown 8–12 hr Unknown

Mechanism of Action

Activates the glucagon-like peptide-1 site on pancreatic beta cells, which increases intracellular cyclic AMP, which increases insulin release when blood glucose level is elevated. In addition, because insulin and glucagon levels occur in an inverse relationship to plasma glucose level, increased insulin level will decrease glucagon level, which inhibits glucagon stimulation of the liver that increases plasma glucose level. Although its exact mechanism is unclear, liraglutide 596 liraglutide also delays gastric emptying, which helps prevent a sudden rise in plasma glucose level after eating. Together these actions work to lower plasma glucose level.

Contraindications

History or presence of medullary thyroid cancer or multiple endocrine neoplasia syndrome type 2, hypersensitivity to liraglutide or its components, ketoacidosis, type 1 diabetes mellitus

Interactions

oral hypoglycemic agents such as sulfonylureas: Increased risk of hypoglycemia orally administered : Possibly decreased absorption of these

Side Efect

CNS: Dizziness, fatigue, headache
CV: Hypertension
EENT: Nasopharyngitis, sinusitis
ENDO: Elevated calcitonin levels, thyroid C-cell hyperplasia, thyroid cancer
GI: Anorexia, constipation, diarrhea, dyspepsia, nausea, pancreatitis, slowed gastric emptying, vomiting
GU: UTI
MS: Back pain
RESP: Upper respiratory tract infection
SKIN: Urticaria
Other: Angioedema, anti-liraglutide antibodies, influenza

Cautions

Be aware that liraglutide isn’t recommended as first-line therapy for patients with type 2 diabetes mellitus not well controlled with diet and exercise. It also isn’t a substitute for insulin therapy.

Liraglutide shouldn’t be given to a patient with a history of thyroid C-cell tumors, including medullary thyroid carcinoma, or to patients with multiple endorcrine neoplasia syndrome type 2 because drug may stimulate tumor growth.

Use liraglutide cautiously in patients with a history of pancreatitis because drug can cause pancreatitis and in patients with impaired hepatic or renal function because drug effects in these patients are unknown.

Dosage of liraglutide given during first week of therapy isn’t enough to provide glycemic control but is given to minimize adverse effects when dosage is increased.

Monitor patient’s serum calcitonin levels, as indicated. Be aware that elevations occur more often when liraglutide dosage is 1.8 mg daily.

Monitor patient for pancreatitis, especially when therapy starts or dosage increases. Report persistent severe abdominal pain; it may radiate to the back and may be accompanied by vomiting. If pancreatitis is confirmed, expect to stop drug and not restart it after episode has been resolved.

Monitor patient for hypoglycemia, especially if he takes another antidiabetic, such as a sulfonylurea. Report any episode of hypoglycemia because dosage of other antidiabetic may need adjustment. Treat hypoglycemia with a glucose-containing food or beverage or give glucagons, as ordered, to raise blood glucose level.

Monitor patient’s blood glucose level and hemoglobin A1Cregularly, as ordered to assess effectiveness of drug.

Monitor effectiveness of all other oral because liraglutide slows gastric emptying and may impair their absorption. Alert prescriber to any concerns.

PATIENT SAFTY

Teach patient how to use prefilled multidose pen and how to give a subcutaneous injection. Explain that he’ll need to inject drug daily but that he can do it at any time of day, independent of meals. Tell patient to inject drug into his abdomen, thigh, or upper arm and to rotate sites to minimize injection site reactions.

Advise patient of possible risk of medullary thyroid cancer and need to report any symptoms, such as a neck mass, dysphagia, dyspnea, or persistent hoarseness.

Stress that liraglutide therapy isn’t a substitute for diet and exercise but is used to enhance effectiveness of these measures.

Category

Chemical class: Sympathomimetic amine
Therapeutic class: CNS stimulant

Pregnancy category: C

Indications

To treat attention deficit hyperactivity disorder (ADHD) Adults and children ages 6 to 12. Initial: 30 mg once daily in the morning, increased as needed in increments of 10 or 20 mg daily every wk. Maximum: 70 mg daily. Route Onset Peak Duration P.O. Unknown 1 hr Unknown

Mechanism of Action

Produces CNS stimulant effects, probably by facilitating release and blocking reuptake of norepinephrine at adrenergic nerve terminals and by stimulating alpha and beta receptors in peripheral nervous system. The drug also releases and blocks reuptake of dopamine in limbic regions of brain. These actions cause decreased motor restlessness and increased alertness.

Contraindications

Advanced arteriosclerosis; agitation; glaucoma; history of drug abuse, hypersensitivity, or idiosyncratic reaction to lisdexamfetamine, other sympathomimetic amines, or their components; hyperthyroidism; MAO inhibitor therapy within 14 days; moderate to severe hypertension; symptomatic cardiovascular disease; history of seizures

Interactions

adrenergic blockers: Inhibited adrenergic blockade acetazolamide, alkalinizers (such as sodium bicarbonate), some thiazides: Increased blood level and effects of lisdexamfetamine antihistamines: Possibly reduced sedation from antihistamine antihypertensives: Possibly decreased antihypertensive effects chlorpromazine: Inhibited CNS stimulant effects of lisdexamfetamine ethosuximide: Possibly delayed ethosuximide absorption GI acidifiers (such as ascorbic acid), reserpine: Decreased amphetamine absorption guanethine: Decreased antihypertensive effect and decreased lisdexamfetamine absorption
haloperidol: Decreased CNS stimulation lithium carbonate: Possibly decreased anorectic and stimulant effects of lisdexamfetamine
MAO inhibitors: Potentiated effects of lisdexamfetamine, possibly hypertensive crisis meperidine: Increased analgesia methenamine: Increased urine excretion and decreased effects of lisdexamfetamine norepinephrine: Possibly increased adrenergic effect of norepinephrine phenobarbital,
phenytoin: Synergistic anticonvulsant action propoxyphene: Increased CNS stimulation, potentially fatal seizures sympathomimetic : Increased stimulant effect tricyclic antidepressants: Possibly increased antidepressant effects and decreased lisdexamfetamine effects urinary acidifiers (such as ammonium chloride and sodium acid phosphate): Increased amphetamine excretion and decreased amphetamine blood level and effects veratrum alkaloids: Decreased hypotensive effect

Side Efect

CNS: Affect lability, aggression, agitation, anxiety, dizziness, fever, hallucinations, headache, insomnia, irritability, jittery feeling, mania, psychomotor hyperactivity, psychotic episodes, seizures, somnolence, tic, tremor
CV: Hypertension, tachycardia, ventricular hyperthrophy
EENT: Blurred vision, dry mouth
GI: Anorexia, diarrhea, nausea, vomiting, upper abdominal pain
GU: Decreased libido, erectile dysfunction
RESP: Dyspnea
SKIN: Diaphoresis, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, physical or psychological dependence, weight loss

Cautions

WARNING Chest pain or fainting should be reported to presciber immediately.
WARNING Lisdexamfetamine shouldn’t be given to patients with structural cardiac abnormalities, cardiomyopathy, or other serious heart problems or rhythm abnormalities because even usual CNSlisdexamfetamine dimesylate 598 stimulant dosages increase risk of sudden death in patients with these conditions.

Use lisdexamfetamine cautiously in patients with hypertension, heart failure, recent MI, or ventricular arrhythmia because drug may increase blood pressure and worsen these conditions.

Monitor patient’s blood pressure closely; stimulant such as lisdexamfetamine may increase it.

Monitor patients with psychosis, bipolar illness, or a history of aggression or hostility; CNS stimulation may worsen symptoms.

Assess growth pattern in pediatric patients because stimulants such as lisdexamfetamine may suppress growth. If so, notify prescriber and expect therapy to be halted.

If patient has a history of seizures or EEG abnormality, watch for seizure activity because stimulants may lower seizure threshold. Rarely, lisamfetamine may cause seizures in a patient with no history of them. Take seizure precautions in all patients, and notify prescriber if a seizure occurs. Expect to discontinue lisdexamfetamine, as prescribed.

Take safety precautions because stimulants may alter accommodation and cause blurred vision. Although these effects haven’t been reported with lisdexamfetamine, the drug is a known stimlulant.

Be aware that therapy may be stopped temporarily to assess continued need for it, as evidenced by a return of hyperactivity and attention deficit.

PATIENT SAFTY

WARNING Tell patient with symptoms such as chest pain or fainting to contact presciber immediately.

Warn patient or caregiver that drug must be taken exactly as prescribed and dosage increased only at prescriber’s instruction because drug can be abused or lead to dependence.

Instruct patient or caregiver that capsule may be opened and contents dissolved in a glass of water and drunk immediately.

Tell patient or caregiver that drug should only be taken in the morning because taking it later in the day may cause insomnia.

Advise patient or caregiver to report any symptoms that suggest heart disease, such as such as exertional chest pain or unexplained syncope.

Urge patient to avoid hazardous activities until drug effects are known.

Tell female patient of childbearing age to notify prescriber if pregnancy is suspected.

Category

Chemical class: Lysine ester of enalaprilat
Therapeutic class: Antihypertensive, vasodilator

Pregnancy category: C

(first trimester), D (later trimesters)

Indications

To manage uncomplicated essential hypertension
Adults. Initial: 10 mg daily. Maintenance: 20 to 40 mg daily. Maximum: 80 mg daily.
DOSAGE ADJUSTMENT For patients with renal failure, initial dosage reduced to 5 mg daily if creatinine clearance is 10 to 30 ml/ min/1.73 m2and to 2.5 mg daily if creatinine clearance is less than 10 ml/min/ 1.73 m2. For patients receiving a diuretic, initial dosage reduced to 5 mg daily. Children age 6 and over with a GFR of at least 30 ml/min/1.73 m2.Initial: 0.07 mg/ kg daily, adjusted according to blood pressure response up to 5 mg daily. Maximum: 0.61 mg/kg or 40 mg daily. To treat heart failure, along with digoxin and diuretics
Adults. Initial: 5 mg daily. Maintenance: 5 to 20 mg daily. Maximum: 80 mg daily.
DOSAGE ADJUSTMENT For patients with hyponatremia or creatinine clearance of 30 ml/min/1.73 m2or less, initial dosage reduced to 2.5 mg daily. To improve survival in hemodynamically stable patient after acute MI
Adults. 5 mg within 24 hr after onset of symptoms, followed by 5 mg after 24 hr and 10 mg after 48 hr. Maintenance: 10 mg daily for 6 wk. Maximum: 80 mg daily.
DOSAGE ADJUSTMENT For patients with baseline systolic blood pressure of 120 mm Hg or less, initial dosage decreased to 2.5 mg daily for first 3 days after MI. If systolic blood pressure falls to 100 mm Hg or less during therapy, maintenance dosage decreased to 2.5 to 5 mg as tolerated; if systolic blood pressure is 90 mm Hg or less for more than 1 hr, drug is discontinued. Route Onset Peak Duration P.O. 1 hr 6–8 hr 24 hr

Mechanism of Action

May reduce blood pressure by inhibiting conversion of angiotensin I to angiotensin II. Angiotensin II is a potent vasoconstrictor that also stimulates adrenal cortex to secrete aldosterone. Lisinopril may also inhibit renal and vascular production of angiotensin II. Decreased release of aldosterone reduces sodium and water reabsorption and increases their excretion, thereby reducing blood pressure.

Contraindications

Hypersensitivity to lisinopril, other ACE inhibitors, or their components; history of angioedema related to previous treatment with an ACE inhibitor; hereditary or idiopathic angioedema

Interactions

allopurinol, bone marrow depressants (such as methotrexate), procainamide, systemic corticosteroids: Increased risk of potentially fatal neutropenia or agranulocytosis cyclosporine, potassium-sparing diuretics, potassium supplements: Increased risk of hyperkalemia diuretics, other antihypertensives: Increased hypotensive effect insulin, oral antidiabetics: Increased risk of hypoglycemia lithium: Increased blood lithium level and risk of lithium toxicity
NSAIDs: Possibly reduced antihypertensive effect, reduced renal function in patients with preexisting renal dysfunction sympathomimetics: Possibly reduced antihypertensive effect high-potassium diet, potassium-containing salt substitutes: Increased risk of hyperkalemia
alcohol use: Possibly increased hypotensive effect

Side Efect

CNS: Ataxia, confusion, depression, dizziness, fatigue, headache, mood alterations, nervousness, stroke, syncope, transient ischemic attack, vertigo
CV: Arrhythmias, chest pain, hypotension, MI, orthostatic hypotension, palpitations, peripheral edema, vasculitis
ENDO: Hyperglycemia, syndrome of inappropriate ADH secretion
EENT: Olfactory disturbance
GI: Abdominal pain, anorexia, cholestatic jaundice, diarrhea, elevated liver enzyme levels, fulminant hepatic necrosis, gastritis, hepatitis, indigestion, nausea, pancreatitis, vomiting
GU: Acute renal failure, decreased libido, impotence, pyelonephritis
HEME: Agranulocytosis, anemia, hemolytic anemia, neutropenia, thrombocytopenia
MS: Muscle spasms, myalgia
RESP: Bronchospasm, cough, dyspnea, paroxysmal nocturnal dyspnea, pulmonary embolism and infarction, upper respiratory tract infection
SKIN: Alopecia, cutaneous pseudolymphoma, diaphoresis, erythema, flushing, herpes zoster, infections, pemphigus, photosensitivity, pruritus, rash, StevensJohnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema

Cautions

Use lisinopril cautiously in patients with fluid volume deficit, heart failure, impaired renal function, or sodium depletion.

To prepare pediatric suspension, add 10 ml purified water to a polyethylene terephthalate (PET) bottle containing ten 20-mg tablets and shake for at least 1 minute. Add 30 ml of Bicitra diluent and 160 ml of Ora-Sweet SF to concentrate in PET bottle and shake gently for several seconds. Refrigerate up to 4 weeks. Shake suspension before each use.

Monitor blood pressure often, especially early in treatment. If excessive hypotension develops, expect to withhold drug for several days.
WARNING If angioedema affects face, glottis, larynx, limbs, lips, mucous memlisinopril 600 branes, or tongue, notify prescriber immediately and expect to stop lisinopril and start appropriate therapy at once. If airway obstruction threatens, promptly give 0.3 to 0.5 ml of epinephrine 1:1,000 solution subcutaneously, as prescribed.

Monitor patient for anaphylaxis, especially patient being dialyzed with high-flux membranes and treated with an ACE inhibitor such as lisinopril. If anaphylaxis occurs, stop dialysis immediately and treat aggressively (antihistamines are ineffective in this situation), as ordered. Anaphylaxis has also occurred with some patients undergoing low-density lipoprotein apheresis with dextran sulfate absorption.

Notify prescriber if patient has persistent, nonproductive cough, a common adverse effect of ACE inhibitors such as lisinopril.

Monitor for dehydration, which can lead to hypotension. Be aware that diarrhea and vomiting can cause dehydration.

Monitor patient for hepatic dysfunction because lisinopril, an ACE inhibitor, may rarely cause a syndrome that starts with cholestatic jaundice or hepatitis and progresses to fulminant hepatic necrosis. If patient develops jaundice or a marked elevation in liver enzyme levels, withhold drug and notify prescriber.

If patient takes insulin or an oral antidiabetic, monitor blood glucose level closely because risk of hypoglycemia increases, especially during first month of therapy.

PATIENT SAFTY

Explain that lisinopril helps to control but doesn’t cure hypertension and that patient may need lifelong therapy.

Advise patient to take lisinopril at the same time every day.

Emphasize need to take drug as ordered, even if patient feels well; caution her not to stop drug without consulting prescriber.

Instruct patient to report dizziness, especially during first few days of therapy.

Inform patient that persistent, nonproductive cough may develop during lisinopril therapy. Urge her to notify prescriber immediately if cough becomes difficult to tolerate.

Advise patient to drink adequate fluid and avoid excessive sweating, which can lead to dehydration and hypotension. Make sure she understands that diarrhea and vomiting also can cause hypotension.

Caution patient not to use salt substitutes that contain potassium.

Instruct patient to report signs of infection, such as fever and sore throat, which may indicate neutropenia.

Advise patient to change position slowly to minimize orthostatic hypotension.

If patient has diabetes and takes insulin or an oral antidiabetic, urge her to monitor her blood glucose level closely and watch for symptoms of hypoglycemia.

Caution female patient to notify prescriber immediately if she is or could be pregnant.

Category

Chemical class: Alkaline metal, monovalent cation
Therapeutic class: Antidepressant, antimanic

Pregnancy category: D

Indications

To treat recurrent bipolar affective disorder, to prevent bipolar disorder depression , Adults and children age 12 and over.Initial: 300 to 600 mg t.i.d. Maintenance: 300 mg t.i.d. or q.i.d. Maximum: 2,400 g daily. Children up to age 12. 15 to 20 mg/kg daily in divided doses b.i.d. or t.i.d. Adults and children age 12 and over. Initial: 900 to 1,800 mg daily in divided doses b.i.d. or t.i.d. Maintenance: 450 mg b.i.d. or 300 mg t.i.d. Maximum: 2,400 g daily. SLOW-RELEASE Adults and children age 12 and over.600 to 900 mg on day 1, increased to 1,200 to 1,800 mg daily in divided doses t.i.d. Maintenance: 900 to 1,200 mg daily in divided doses t.i.d. Maximum: 2,400 g daily. SYRUP (LITHIUM CITRATE) Adults and children age 12 and over. 8 to 16 mEq (equivalent of 300 to 600 mg of lithium carbonate) t.i.d. Maintenance: Equivalent of 300 mg of lithium carbonate t.i.d. or q.i.d. Maximum: Equivalent of 2,400 g daily of lithium carbonate. Children up to age 12. 0.4 to 0.5 mEq (equivalent of 15 to 20 mg of lithium carbonate)/ kg daily in divided doses b.i.d. or t.i.d. Route Onset Peak Duration P.O. 1–3 wk Unknown Unknown

Mechanism of Action

May increase presynaptic degradation of the catecholamine neurotransmitters serotonin, dopamine, and norepinephrine; inhibit their release at neuronal synapses; and decrease postsynaptic receptor sensitivity. These actions may correct overactive catecholamine systems in patients with mania. Antidepressant action may result from enhanced serotonergic activity.

Contraindications

Blood dyscrasias, bone marrow depression, brain damage, cerebrovascular disease, coma, coronary artery disease, excessive intake of other CNS depressants, hypersensitivity to lithium or its components, impaired hepatic function, myeloproliferative disorders, severe depression, severe hypertension or hypotension

Interactions

ACE inhibitors, NSAIDs, piroxicam: Possibly increased blood lithium level and increased risk of toxicity acetazolamide, sodium bicarbonate, urea, xanthines: Decreased blood lithium level calcium channel blockers, molindone: Increased risk of neurotoxicity from lithium calcium iodide, iodinated glycerol, potassium iodide: Possibly increased hypothyroid effects of both carbamazepine: Possibly increased therapeutic effects of carbamazepine and neurotoxic effect of lithium chlorpromazine, other phenothiazines: Possibly impaired GI absorption and decreased blood levels of these ; possibly masking of early signs of lithium toxicity desmopressin, lypressin, vasopressin: Possibly impaired antidiuretic effects of these diuretics (loop and osmotic): Increased lithium reabsorption by kidneys, possibly leading to lithium toxicity fluoxetine, methyldopa, metronidazole: Increased risk of lithium toxicity from reduced renal clearance of lithiun haloperidol and other antipyschotics: Increased risk of irreversible neurotoxicity and brain damage neuromuscular blockers: Risk of prolonged paralysis or weakness norepinephrine: Possibly decreased therapeutic effects of norepinephrine and severe respiratory depression selective serotonin reuptake inhibitors: Increased risk of adverse effects, such as diarrhea, confusion, dizziness, agitation, and tremor thyroid hormones: Possibly hypothyroidism tricyclic antidepressants: Possibly severe mood swings from mania to depression high-sodium : Increased excretion and possibly decreased therapeutic effects of lithium

Side Efect

CNS: Ataxia, coma, confusion, depression, dizziness, drowsiness, headache, lethargy, seizures, syncope, tremor (in hands), vertigo
CV: Arrhythmias (including bradycardia and tachycardia), ECG changes, edema
EENT: Dental caries, dry mouth, exophthalmos
ENDO: Diabetes insipidus, euthyroid goiter, hypothyroidism, myxedema
GI: Abdominal distention and pain, anorexia, diarrhea, nausea, thirst
GU: Stress incontinence, urinary frequency
HEME: Leukocytosis
MS: Muscle twitching and weakness
RESP: Dyspnea
SKIN: Acne; alopecia; dry, thin hair; pruritus; rash
Other: Cold sensitivity, weight gain or loss

Cautions

Administer lithium after meals to slow absorption from GI tract and reduce

Side Efect

. Dilute syrup with juice lithium 602 or other flavored drink before giving.

Note that 5 ml of lithium citrate equals 8 mEq of lithium ion or 300 mg of lithium carbonate.

Expect to monitor blood lithium level two or three times weekly during first month, and then weekly to monthly during maintenance therapy and when starting or stopping NSAID therapy. In uncomplicated cases, plan to monitor lithium level every 2 to 3 months.

Be aware that lithium has a narrow therapeutic range. Even a slightly high blood level is dangerous, and some patients show signs of toxicity at normal levels.

Expect prescriber to decrease dosage after acute manic episode is controlled.
WARNING Be aware that lithium affects intracellular and extracellular potassium ion shift, which can cause ECG changes, such as flattened or inverted T waves; it also can increase the risk of cardiac arrest.

Monitor ECGs, renal and thyroid function test results, and serum electrolyte levels, as appropriate, during lithium treatment.
WARNING Be aware that lithium can cause reversible leukocytosis, which usually peaks within 7 to 10 days of starting therapy; WBC count typically returns to baseline within 10 days after therapy stops.

Weigh patient daily to detect sudden weight changes.

Monitor blood glucose level often in diabetic patient because lithium alters glucose tolerance.

Palpate thyroid gland to detect enlargement because drug may cause goiter.

Ensure that patient’s fluid and sodium intake is adequate during treatment.

PATIENT SAFTY

Advise patient to take lithium with or after meals to minimize

Side Efect

.

Instruct patient to swallow or slowrelease form whole.

Direct patient to mix syrup form with juice or other flavored drink before taking.

Inform patient that frequent urination, nausea, and thirst may occur during the first few days of treatment.

Caution patient not to stop taking lithium or adjust dosage without first consulting prescriber.

Instruct patient to report signs of toxicity, such as diarrhea, drowsiness, muscle weakness, tremor, uncoordinated body movements, and vomiting.

Urge patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to maintain normal fluid and sodium intake.

Emphasize importance of complying with scheduled checkups and laboratory tests.

Category

Chemical class: Fluoroquinolone
Therapeutic class: Antibiotic

Pregnancy category: C

Indications and Dosage To treat mild to moderate lower respiratory tract infections caused by susceptible organisms, including Haemophilus influenzae and Moraxella catarrhalis
Adults. 400 mg daily for 10 days. To treat uncomplicated cystitis caused by Escherichia coli; to treat uncomplicated cystitis caused by Klebsiella pneumoniae, Proteus mirabilis, or Staphylococcus saprophyticus
Adults. 400 mg daily for 3 days. To treat complicated UTI caused by Citrobacter diversus, Enterobacteriaceae, E. coli, K. pneumoniae, P. mirabilis, or Pseudomonas aeruginosa
Adults. 400 mg daily for 14 days. To provide prophylaxis for transurethral surgery
Adults.400 mg as a single dose 2 to 6 hr before surgery. To provide prophylaxis for transrectal biopsy
Adults. 400 mg as a single dose 1 to 6 hr before surgery. To treat gonorrhea (as alternative to ciprofloxacin or ofloxacin)
Adults. 400 mg as a single dose.
DOSAGE ADJUSTMENT For patients with creatinine clearance between 11 and 39 ml/ min/1.73 m2, loading dose of 400 mg given on day 1 and followed by 200 mg daily.

Mechanism of Action

Inhibits the bacterial enzyme DNA gyrase, which normally is responsible for unwinding and supercoiling of bacterial DNA before it replicates. By inhibiting this enzyme, lomefloxacin interferes with bacterial cell replication and causes cell death.

Contraindications

History of tendinitis or tendon rupture, hypersensitivity to lomefloxacin or any quinolone derivative

Interactions

aluminum-, calcium-, or magnesiumcontaining antacids; iron salts; sucralfate; zinc: Decreased absorption and blood level of lomefloxacin cyclosporine: Possibly increased blood cyclosporine level, increased nephrotoxicity probenecid: Decreased lomefloxacin excretion, increased risk of toxicity
warfarin: Possibly increased anticoagulant effect and risk of bleeding

Side Efect

CNS: Ataxia, cerebral thrombosis, dizziness, drowsiness, hallucinations, headache, insomnia, nervousness, peripheral neuropathy, phobia, vertigo
CV: Prolonged QT interval, torsades de pointes, vasculitis
EENT: Diplopia, laryngeal edema, oral candidiasis, painful oral mucosa, taste perversion
GI: Abdominal pain, diarrhea, hepatitis, indigestion, nausea, pseudomembranous colitis, vomiting
GU: Interstitial nephritis, polyuria, renal failure, urine retention, vaginal candidiasis
HEME: Hemolytic anemia
MS: Tendinitis, tendon rupture
RESP: Pulmonary edema
SKIN: Exfolitaive dermatitis, hyperpigmentation, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis

Cautions

Know that lomefloxacin shouldn’t be given to patients with QT-interval prolongation or hypokalemia or to patients taking class IA antiarrhythmics (such as quinidine or procainamide) or class III antiarrhythmics (such as amiodarone or sotalol) because of increased risk of torsades de pointes.

Expect to obtain body fluid or tissue sample for culture and sensitivity testing and to review results, if possible, before lomefloxacin therapy begins.

If patient’s culture test results are positive for gonorrhea, expect to obtain serologic test for syphilis at diagnosis and to repeat test 3 months after lomefloxacin therapy.

Give drug with meals and a full glass of water.

Ensure that patient maintains adequate fluid intake during therapy.

Monitor for evidence of secondary infections, such as sore mouth or vaginal discharge.

Notify prescriber if patient experiences severe or prolonged diarrhea, which may indicate pseudomembranous colitis.

Be aware that prolonged use may lead to growth of drug-resistant organisms.

Notify prescriber and expect to stop lomefloxacin if patient develops symptoms of peripheral neuropathy (pain, burning, tingling, numbness, weakness, or changes in sensations of light touch, pain, temperature, position, or vibration) to prevent an irreversible condition or tendon rupture that requires immediate rest and avoidance of exercise involving affected area.

PATIENT SAFTY

Advise patient to take lomefloxacin at same time each day with meals and with a full glass of water.

Caution patient not to take antacids, iron, sucralfate, or zinc 1 hour before or 2 hours after taking lomefloxacin because these preparations impair drug absorption.

Urge patient to drink plenty of fluids during treatment.

Instruct patient to complete full course of therapy, even if symptoms subside.

Advise patient to notify prescriber if symptoms don’t improve within a few days after starting lomefloxacin or if severe GI distress or diarrhea develops.

Instruct patient to notify prescriber and stop taking drug if she has tendon inflamlomefloxacin hydrochloride 604 mation or pain; advise her to rest until tendinitis and tendon rupture have been ruled out.

Urge patient to avoid direct sunlight, to wear protective clothing, and to use sunscreen because photosensitivity reactions can occur during therapy and for several days afterward.

Explain that risk of photosensitivity can be decreased by taking lomefloxacin at least 12 hours before sun exposure. Urge patient to stop drug and notify prescriber at first sign of photosensitivity, such as skin burning, redness, swelling, blisters, rash, itching, or dermatitis.

Inform patient that an allergic reaction may occur after a single dose. Tell patient to stop lomefloxacin and notify prescriber if rash or other allergic reaction develops.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Category

Chemical class: Carbacephem
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat acute bronchitis caused by Haemophilus influenzae, Moraxella catarrhalis, or Streptococcus pneumoniae , ORAL SUSPENSION Adults and adolescents. 200 to 400 mg every 12 hr for 7 days. To treat chronic bronchitis exacerbations caused by H. influenzae, M. catarrhalis, or S. pneumoniae , ORAL SUSPENSION Adults and adolescents. 400 mg every 12 hr for 7 days. To treat pneumonia caused by H. influenzae or S. pneumoniae , ORAL SUSPENSION Adults and adolescents. 400 mg every 12 hr for 14 days. To treat pharyngitis, sinusitis, or tonsillitis caused by Streptococcus pyogenes , ORAL SUSPENSION Adults and adolescents. 200 to 400 mg every 12 hr for 10 days. Children.7.5 mg/kg every 12 hr for 10 days. To treat acute otitis media caused by H. influenzae, M. catarrhalis, S. pneumoniae, or S. pyogenes ORAL SUSPENSION Children.15 mg/kg every 12 hr for 10 days. To treat uncomplicated skin and softtissue infections caused by Staphylococcus aureus or S. pyogenes , ORAL SUSPENSION Adults and adolescents. 200 mg every 12 hr for 7 days. ORAL SUSPENSION Children. 7.5 mg/kg every 12 hr for 7 days. To treat uncomplicated cystitis caused by Escherichia coli or Staphylococcus saprophyticus , ORAL SUSPENSION Adults and adolescents. 200 mg daily for 7 days. To treat uncomplicated pyelonephritis caused by E. coli , ORAL SUSPENSION Adults and adolescents. 400 mg every 12 hr for 14 days.
DOSAGE ADJUSTMENT If creatinine clearance is 10 to 49 ml/min/1.73 m2, 50% of usual dose given at normal interval or usual dose given at twice the normal interval; if clearance is less than 10 ml/min/1.73 m2, usual adult dosage given every 3 to 5 days.

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting final step in the cross-linking of peptidoglycan strands. Peptidoglycan makes bacterial cell membrane rigid and protective. Without it, bacterial cells rupture and die.

Contraindications

Hypersensitivity to loracarbef, other cephalosporins, or their components

Interactions

probenecid: Inhibited renal excretion of loracarbef, resulting in increased blood level all : Inhibited drug absorption

Side Efect

CNS: Dizziness, drowsiness, headache, insomnia, nervousness, seizures
EENT: Oral candidiasis
GI: Abdominal pain,anorexia,diarrhea,nausea,pseudomembranous colitis,vomiting
GU: Vaginal candidiasis
SKIN: Pruritus, rash, urticaria

Cautions

Expect to obtain body fluid or tissue sample for culture and sensitivity testing and to review results, if possible, before giving first dose of loracarbef.

Be aware that oral suspension is absorbed more rapidly and produces a higher peak plasma level than capsules.

Monitor patient for signs of secondary infections, such as sore mouth and vaginal discharge.

Watch for seizures, especially if patient has impaired renal function.

PATIENT SAFTY

Advise patient to take loracarbef at least 1 hour before or 2 hours after meals.

Tell patient to complete full course of drug as prescribed, even if symptoms decrease.

Instruct patient to discard unused oral solution after 14 days.

Advise patient to report diarrhea, hives, or severe rash to prescriber.

Category

Chemical class: Benzodiazepine
Therapeutic class: Amnestic, antianxiety, anticonvulsant, sedative

Pregnancy category: D

(parenteral), Not rated (oral) Controlled substance schedule: IV

Indications

To treat anxiety ORAL CONCENTRATE, Adults and adolescents. 1 to 3 mg b.i.d. or t.i.d. Maximum: 10 mg daily.
DOSAGE ADJUSTMENT For elderly or debilitated patients, initial dosage may be reduced to 0.5 to 2 mg daily in divided doses. To treat insomnia caused by anxiety ORAL CONCENTRATE, Adults and adolescents. 2 to 4 mg at bedtime.
DOSAGE ADJUSTMENT Dosage possibly reduced for elderly or debilitated patients. To provide preoperative sedation
I.V.INJECTION Adults and adolescents. 0.044 mg/kg or 2 mg, whichever is less, given 2 hr before procedure. Maximum: 0.05 mg/kg or total of 4 mg.
I.M.INJECTION Adults and adolescents. 0.05 mg/kg 2 hr before procedure. Maximum: 4 mg. To treat status epilepticus
I.V.INJECTION Adults and adolescents. Initial: 4 mg at a rate of 2 mg/min. Repeated in 10 to 15 min if seizures don’t subside. Maximum: 8 mg/ 24 hr. Route Onset Peak Duration I.V. 5 min Unknown 12–24 hr I.M. 15–30 min Unknown 12–24 hr

Mechanism of Action

May potentiate the effects of gammaaminobutyric acid (GABA) and other inhibitory neurotransmitters by binding to specific benzodiazepine receptors in limbic and cortical areas of CNS. GABA inhibits excitatory stimulation, which helps control emotional behavior. Limbic system contains a highly dense area of benzodiazepine receptors, which may explain drug’s antianxiety effects. Also, lorazepam hyperpolarizes neuronal cells, thereby interfering with their ability to generate seizures.

Incompatibilities

Don’t mix I.V. lorazepam in same syringe as buprenorphine.

Contraindications

Acute angle-closure glaucoma, hypersensitivity to lorazepam, its components, or benzodiazepines; intra-arterial delivery; psychosis

Interactions

aminophylline,
theophylline: Possibly reduced sedative effects of lorazepam clozapine: Increased risk of marked sedation, excessive salivation, hypotension, ataxia, delirium, and respiratory arrest
CNS depressants: Additive CNS depression, potentially fatal respiratory depression digoxin: Possibly increased blood digoxin level and risk of digitalis toxicity fentanyl: Possibly decreased therapeutic effects of fentanyl probenecid: Possibly increased therapeutic and adverse effects of lorazepam
alcohol use: Increased CNS depression

Side Efect

CNS: Amnesia, anxiety, ataxia, coma, confusion, delusions, depression, dizziness, drowsiness, euphoria, extrapyramidal symptoms, fatigue, headache, hypokinesia, irritability, malaise, nervousness, seizures, slurred speech, suicidal ideation, tremor, unsteadiness, vertigo
CV: Chest pain, palpitations, tachycardia
EENT: Blurred vision, diplopia, dry mouth, increased salivation, photophobia
ENDO: Syndrome of inappropriate ADH
GI: Abdominal pain, constipation, diarrhea, increased liver enzyme levels, jaundice, nausea, thirst, vomiting
GU: Libido changes
HEME: Agranulocytosis, pancytopenia, thrombocytopenia
RESP: Apnea, respiratory depression, worsening of sleep apnea or obstructve pulmonary disease
SKIN: Diaphoresis
Other: Anaphylaxis, injection site pain (I.M.) or phlebitis (I.V.), physical and psychological dependence, withdrawal symptoms

Cautions

Before starting lorazepam therapy in a patient with depression, make sure he already takes an antidepressant because of increased risk of suicide in patients with untreated depression.

Use extreme caution when giving lorazepam to elderly patients, especially those with compromised respiratory function, because drug can cause hypoventilation, sedation, unsteadiness, and respiratory depression.

Use drug cautiously in patients with a history of alcohol or drug abuse or a personality disorder because of an increased risk of physical and psychological dependence. Also use cautiously in patients with severe hepatic insufficiency or encephalopathy because drug may worsen hepatic encephalopathy.

For I.M. use, inject lorazepam deep into large muscle mass, such as gluteus maximus.

For I.V. use, dilute lorazepam with equal amount of sterile water for injection, sodium chloride for injection, or D5W. Give diluted lorazepam slowly, at no more than 2 mg/min.

During I.V. use, monitor patient’s respirations every 5 to 15 minutes and keep emergency resuscitation equipment readily available.
WARNING Monitor patient’s respiratory status closely because drug may cause lifethreatening respiratory depression.

Because stopping drug abruptly increases risk of withdrawal symptoms, expect to taper dosage gradually, especially in epileptic patients.

PATIENT SAFTY

Instruct patient to take lorazepam exactly as prescribed and not to stop without consulting prescriber because of risk of withdrawal symptoms.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Urge patient to avoid alcohol while taking lorazepam because it increases drug’s CNS depressant effects.

Instruct patient to report excessive drowsiness and nausea.

Inform pregnant patient that lorazepam therapy will need to be discontinued early in third trimester to avoid possible withdrawal symptoms in newborn.

Category

Chemical class: Angiotensin II receptor antagonist
Therapeutic class: Antihypertensive

Pregnancy category: C

(first trimester), D (later trimesters)

Indications

To manage hypertension
Adults. Initial: 50 mg daily. Maintenance: 25 to 100 mg as a single dose or in divided doses b.i.d. To treat nephropathy in patients with type 2 diabetes and hypertension
Adults. Initial: 50 mg daily, increased to 100 mg daily, as needed. To reduce stroke risk in patients with hypertension and left ventricular hypertrophy
Adults. Initial: 50 mg daily, followed by 12.5 mg hydrochlorothiazide daily. Dosage increased to 100 mg daily, as needed, followed by 25 mg hydrochlorothiazide daily, as needed. Children age 6 and over. Initial: 0.7 mg/kg to a maximum of 50 mg daily. Maximum: 1.4 mg/kg or 100 mg daily.
DOSAGE ADJUSTMENT Initial losartan dosage reduced to 25 mg daily for patients with impaired hepatic function or volume depletion. Route Onset Peak Duration P.O. Unknown 6 hr Over 24 hr

Mechanism of Action

Blocks binding of angiotensin II to receptor sites in many tissues, including vascular smooth muscle and adrenal glands. Angiotensin II is a potent vasoconstrictor that also stimulates the adrenal cortex to secrete aldosterone. The inhibiting effects of angiotensin II reduce blood pressure.

Contraindications

Hypersensitivity to losartan or its components

Interactions

antihypertensives, diuretics: Possibly hypotension cyclosporine, potassium-sparing diuretics, potassium supplements: Increased risk of hyperkalemia indomethacin, sympathomimetics: Possibly decreased antihypertensive effect of losartan
NSAIDs: Possibly decreased renal function in patients already compromised; possibly decreased effectiveness of losartan high-potassium diet, potassium-containing salt substitutes: Increased risk of hyperkalemia

Side Efect

CNS: Dizziness, fatigue, headache, insomnia, malaise
CV: Hypotension
EENT: Nasal congestion
GI: Diarrhea, indigestion, nausea, vomiting
HEME: Thrombocytopenia
MS: Back pain, leg pain, muscle spasms
RESP: Cough, upper respiratory tract infection
SKIN: Erythroderma
Other: Angioedema, hyperkalemia, hyponatremia

Cautions

In some patients, losartan is more effective when given in two divided doses daily; it may be used with other antihypertensives.

Know that patients of African descent with hypertension and left ventricular hypertrophy may not benefit from losartan to reduce stroke risk.
WARNING Be aware that patients who have severe heart failure or renal artery stenosis may experience acute renal failure from losartan therapy because losartan inhibits the angiotensin-aldosterone system, on which renal function depends.

Monitor blood pressure and renal function studies to evaluate drug effectiveness.

Periodically monitor patient’s serum potassium level, as appropriate, to detect hyperkalemia.

Monitor patient for muscle pain; rarely, rhabdomyolysis develops in patients taking other angiotensin II receptor blockers.

PATIENT SAFTY

Instruct patient to avoid potassiumcontaining salt substitutes because thay may increase risk of hyperkalemia.

Advise patient to avoid exercising in hot weather and drinking excessive amounts of alcohol; instruct her to notify prescriber if she has prolonged diarrhea, nausea, or vomiting.

Category

Chemical class: Mevinic acid derivative
Therapeutic class: Antihyperlipidemic

Pregnancy category: X

Indications

To reduce LDL and total cholesterol levels in patients with primary hypercholesterolemia
Adults.Initial: 20 mg as a single dose with evening meal. Maintenance: 20 to 80 mg daily as a single dose or in divided doses with meals. Maximum: 80 mg daily.
DOSAGE ADJUSTMENT For patients who also take immunosuppressants, initial dosage decreased to 10 mg daily and maximum dosage limited to 20 mg daily.
Adults. Initial: 10 mg, 20 mg, 40 mg, or 60 mg as single dose at bedtime, increased, as needed, every 4 wk, up to maximum dose. Maintenance: 10 to 60 mg daily as single dose. Maximum: 60 mg daily. To reduce LDL, total cholesterol, and apolipoprotein B levels in adolescents with heterozygous familial hypercholesterolemia Adolescents 1 yr postmenarche (ages 10 to 17). Initial: 20 mg daily for LDL reduction of 20% or more, 10 mg daily for LDL reduction of less than 20%; dosage adjusted after at least 4 wk. Maintenance: 10 to 40 mg daily. Maximum: 40 mg daily.
DOSAGE ADJUSTMENT For patients who also take amiodarone or verapamil, maximum dosage limited to 40 mg daily. For patients who also take cyclosporine, gemfibrozil or other fibrates, or lipid-lowering such as niacin (1 g or more daily), maximum dosage of lovastatin limited to 20 mg daily. For patients with creatinine clearance less than 30 ml/min/1.73 m2, maximum dosage limited to 20 mg daily. Route Onset Peak Duration P.O. In 2 wk Unknown 4–6 wk

Mechanism of Action

Interferes with the hepatic enzyme hydroxymethylglutaryl-coenzyme A reductase. By doing so, lovastatin reduces formation of mevalonic acid (a cholesterol precursor), thus interrupting the pathway by which cholesterol is synthesized. When cholesterol level declines in hepatic cells, LDLs are consumed, which also reduces amount of circulating total cholesterol and serum triglycerides. The decrease in LDLs may result in decreased level of apolipoprotein B, which is found in each LDL particle.

Contraindications

Acute hepatic disease, breastfeeding, hypersensitivity to lovastatin or its components, pregnancy, unexplained elevated liver function test results

Interactions

amiodarone, clarithromycin, cyclosporine, danazol, erythromycin, fibric acid derivatives, gemfibrozil and other fibrates, HIV protease inhibitors, immunosuppressants, itraconazole, ketoconazole, nefazodone, niacin (1 g daily or more), telithromycin, verapamil: Increased risk of severe myopathy or rhabdomyolysis bile acid sequestrants, cholestyramine, colestipol: Decreased bioavailability of lovastatin isradipine: Increased hepatic clearance of lovastatin itraconazole,
ketoconazole: Increased lovastatin blood level oral anticoagulants: Increased anticoagulant effect and risk of bleeding all : Increased lovastatin absorption grapefruit juice (more than 1 qt daily): Increased risk of myopathy or rhabdomyolysis
alcohol use: Increased lovastatin blood level

Side Efect

CNS: Dizziness, fatigue, headache, insomnia
EENT: Blurred vision, cataracts, pharyngitis, rhinitis, sinusitis
GI: Abdominal cramps and pain, constipation, diarrhea, elevated liver function test results, flatulence, indigestion, nausea, vomiting
MS: Arthritis, back pain, myalgia, myopathy, myositis, rhabdomyolysis
RESP: Cough, upper respiratory tract infection
SKIN: Dermatomyositis, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, angioedema

Cautions

Give lovastatin cautiously in patients who have a history of liver disease and patients who consume large amounts of alcohol.

Monitor liver function test results before and during therapy. If serum transaminase levels rise, expect to measure them more often, as ordered. If AST or ALT level reaches or exceeds three times upper limit of normal and persists at that level, expect to discontinue lovastatin.

Give drug 1 hour before or 4 hours after bile acid sequestrant, cholestyramine, or colestipol.

Expect patient to be prescribed a standard low-cholesterol diet during therapy.

Be aware that drug affects mainly total cholesterol and LDL levels; it has only slight effects on HDL and triglyceride levels.

PATIENT SAFTY

Tell patient who takes drug once daily to do so with evening meal to enhance absorption.

Advise patient to report muscle aches, pains, tenderness, or weakness; severe GI distress; and vision changes.

Urge patient to avoid consuming alcohol or more than 1 quart of grapefruit juice daily while taking drug.

Direct patient to follow a low-cholesterol diet during therapy. Recommend weight loss and exercise programs as appropriate.

Stress the importance of periodic eye examinations during therapy.

Teach female patients appropriate contraceptive methods and the need to report suspected pregnancy immediately.

Category

Chemical class: Dibenzoxazepine derivative
Therapeutic class: Antipsychotic

Pregnancy category: C

Indications

To treat psychotic disorders and schizophrenia ,
Adults. Initial: 10 mg b.i.d., increased over 7 days. Maintenance: 15 to 25 mg b.i.d. to q.i.d. Maximum: 250 mg daily.
DOSAGE ADJUSTMENT For elderly patients, dosage reduced to 3 to 5 mg b.i.d. To treat acute exacerbations of psychotic disorders
I.M.INJECTION
Adults. 12.5 to 50 mg every 4 to 6 hr or longer. Maximum: 250 mg daily. Route Onset Peak Duration P.O. 20–30 min 1.5–3 hr 12 hr

Mechanism of Action

May treat psychotic disorders by blocking dopamine at postsynaptic receptors in the brain. With prolonged use, loxapine enhances antipsychotic effects by causing depolarization blockade of dopamine tracts, resulting in decreased dopamine neurotransmission.

Contraindications

Blood dyscrasias, bone marrow depression, cerebrovascular disease, coma, coronary artery disease, hypersensitivity to loxapine or its components, impaired hepatic function, myeloproliferative disorders, severe drug-induced CNS depression, severe hypertension or hypotension

Interactions

amphetamines, ephedrine: Decreased effects of these antacids, antidiarrheals (adsorbent): Possibly decreased absorption of oral loxapine anticholinergics: Possibly increased anticholinergic effects anticonvulsants: Lowered seizure threshold, increased risk of seizures antidyskinetics: Possibly antagonized therapeutic effects of these bromocriptine: Possibly decreased therapeutic effects of bromocriptine
CNS depressants: Increased effects of CNS depression dopamine: Possibly decreased alphaadrenergic effects of dopamine epinephrine: Possibly severe hypotension or tachycardia, decreased epinephrine effects guanadrel, guanethidine, levodopa: Possibly decreased therapeutic effects of these MAO inhibitors, tricyclic antidepressants: Possibly increased blood levels of these , increased CNS depressant and anticholinergic effects metaraminol: Possibly decreased vasopressor effect of metaraminol methoxamine: Possibly decreased vasopressor effect and methoxamine duration of action
alcohol use: Increased CNS depression

Side Efect

CNS: Confusion, drowsiness, dystonia, involuntary motor activity, neuroleptic malignant syndrome, pseudoparkinsonism, sleep disturbance, tardive dyskinesia
CV: Orthostatic hypotension
EENT: Blurred vision, dry mouth
ENDO: Galactorrhea, gynecomastia
GI: Constipation, ileus, nausea, vomiting
GU: Menstrual irregularities, sexual dysfunction, urine retention
SKIN: Photosensitivity (mild), rash
Other: Weight gain

Cautions

Be aware that loxapine’s full antipsychotic effect may require weeks.

Loxapine shouldn’t be given to treat dementia-related psychosis in the elderly because of an increased mortality risk.

Assess for signs of tardive dyskinesia, including involuntary protrusion of tongue and chewing movements. These signs may appear months or years after loxapine therapy begins and may not disappear with dosage reduction.

Observe for extrapyramidal reactions or parkinsonian symptoms, such as excessive salivation, masklike facies, rigidity, and tremor, especially in first few days of treatment. Prescriber may reduce dosage to control these symptoms.
WARNING Monitor patient for neuroleptic malignant syndrome, a rare but possibly fatal adverse reaction. Early evidence includes altered mental status, arrhythmias, fever, and muscle rigidity.

PATIENT SAFTY

Instruct patient to dilute loxapine oral solution with orange or grapefruit juice just before taking. Advise her to use calibrated dropper that accompanies solution to ensure correct dosage.

Tell patient not to take antacids and antidiarrheals within 2 hours of loxapine.

Caution patient to avoid alcohol while taking loxapine.

Advise patient to change position slowly to minimize orthostatic hypotension.

Urge patient to avoid hazardous activities until CNS effects of loxapine are known.

Advise patient to avoid prolonged sun exposure and to use sunscreen to minimize risk of photosensitivity.

Urge patient to have periodic eye examinations during therapy.

Category

Chemical class: Chloride channel activator
Therapeutic class: Intestinal motility enhancer

Pregnancy category: C

Indications

To treat chronic idiopathic constipation
Adults.24 mcg b.i.d. with food and water. To treat irritable bowel syndrome with constipation
Adults. 8 mcg b.i.d. with food and water.

Mechanism of Action

Enhances chloride-rich intestinal fluid secretion by locally activating chloride channels. By increasing intestinal fluid secretion, lubiprostone increases intestinal motility, which aids passage of stool, alleviating constipation.

Contraindications

Diarrhea, hypersensitivity to lubiprostone or components, mechanical GI obstruction

Interactions

antidiarrheals: Decreased GI motility

Side Efect

CNS: Asthenia, dizziness, fatigue, headache, malaise
CV: Chest discomfort or pain, edema, increased heart rate
EENT: Dry mouth, throat tightness
GI: Abdominal distention or pain, diarrhea, dyspepsia, flatulence, nausea, vomiting
MS: Muscle cramps or spasms
RESP: Dyspnea
SKIN: Rash
Other: Angioedema

Cautions

Be aware that lubiprostone shouldn’t be used in patients with severe diarrhea.

Make sure woman a negative pregnancy test before starting lubiprostone because safety during pregnancy is unknown.

Watch closely for

Side Efect

,particularly dyspnea and especially after first dose.

PATIENT SAFTY

Advise patient to take drug with food to minimize risk of nausea.

Tell women to use effective contraception while taking lubiprostone and to notify prescriber if pregnancy is suspected. Drug may need to be discontinued.

Instruct patient to notify prescriber if severe diarrhea occurs.

Category

Chemical class: Synthetic vasopressin analogue
Therapeutic class: Antidiuretic

Pregnancy category: C

Indications

To control and prevent dehydration, polydipsia, and polyuria in patients with neurogenic diabetes insipidus that is unresponsive to other therapy NASAL SOLUTION Adults and adolescents. 1 or 2 sprays q.i.d. If more drug is needed, interval between doses is decreased rather than increasing number of sprays/dose.

Mechanism of Action

Increases cellular permeability of collecting ducts in kidneys, leading to increased urine osmolality and decreased urine output.

Contraindications

Hypersensitivity to lypressin or components Route Onset Peak Duration Intranasal In 1 hr 0.5–2 hr 3–4 hr

Interactions

carbamazepine, chlorpropamide, clofibrate: Possibly increased antidiuretic effect demeclocycline, lithium, norepinephrine: Decreased antidiuretic effect of lypressin

Side Efect

CNS: Headache
EENT: Conjunctivitis; nasal congestion, irritation, and itching; periorbital edema and itching; rhinorrhea
GI: Abdominal cramps, diarrhea, heartburn (if excessive intranasal use causes dripping into pharynx)
RESP: Cough, transient dyspnea (if drug is accidentally inhaled)
Other: Water intoxication

Cautions

Assess patient for nasal congestion or upper respiratory tract infection, which can reduce lypressin absorption and require larger doses or adjunct therapy.

Administer final spray of drug at bedtime to help control nocturia.
WARNING Inadvertent inhalation, although rare, may cause chest tightness, continuous cough, and dyspnea.

Observe for nasal irritation during longterm therapy.

Watch for evidence of water intoxication, including coma, confusion, drowsiness, persistent headache, seizures, urine retention, and weight gain.

PATIENT SAFTY

Teach patient how to administer lypressin correctly by holding head upright and bottle in a vertical position and spraying 1 or 2 sprays in each nostril with each dose.

Instruct patient to take last dose of day at bedtime to control nocturia.

Instruct patient to use drug exactly as prescribed.

Tell patient to report abdominal cramps, heartburn, persistent headache, severe nasal irritation, and shortness of breath.

Category

Chemical class: Cation, electrolyte
Therapeutic class: Antacid, antiarrhythmic, anticonvulsant, electrolyte replacement, laxative Pregnancy category: A (parenteral magnesium sulfate), Not rated (others)

Indications

To correct magnesium deficiency caused by alcoholism, magnesium-depleting , malnutrition, or restricted diet; to prevent magnesium deficiency based on U.S. and Canadian recommended daily allowances , CHEWABLE , CRYSTALS, ENTERIC-COATED , , LIQUID, LIQUID CONCENTRATE,, (MAGNESIUM CHLORIDE, CITRATE, GLUCONATE, HYDROXIDE, LACTATE[EXCEPT IN CHILDREN], OXIDE, SULFATE) Dosage individualized based on severity of deficiency and normal recommended daily allowances listed below. Adult men and children over age 10. 270 to 400 mg daily (Canada: 130 to 250 mg daily). Adult women and children over age 10. 280 to 300 mg daily (Canada: 135 to 210 mg daily). Pregnant women. 320 mg daily (Canada: 195 to 245 mg daily). Breast-feeding women.340 to 355 mg daily (Canada: 245 to 265 mg daily). Children ages 7 to 10. 170 mg daily (Canada: 100 to 135 mg daily). Children ages 4 to 6. 120 mg daily (Canada: 65 mg daily). Children from birth to age 3. 40 to 80 mg/ day (Canada: 20 to 50 mg daily). To treat mild magnesium deficiency M M

IM

(MAGNESIUM SULFATE) Adults and adolescents.1 g every 6 hr for 4 doses. To treat severe hypomagnesemia
IV:
Adults. 4 g diluted in 250 ml D5W and infused at no more than 3 ml/min. Maximum: 40 g daily.
IV:(MAGNESIUM SULFATE) Adults and adolescents. 5 g diluted in 1 L I.V. solution and infused over 3 hr. To provide supplemental magnesium in total parenteral nutrition
IV:(MAGNESIUM SULFATE)
Adults. 1 to 3 g daily. Children.0.25 mg to 1.25 g daily.
DOSAGE ADJUSTMENT Adult dosage may be increased to 6 g daily for certain conditions, such as short-bowel syndrome.

IM

Adults and adolescents.Up to 250 mg/kg every 4 hr, p.r.n. To prevent and control seizures in preeclampsia or eclampsia as well as seizures caused by epilepsy, glomerulonephritis, or hypothyroidism
IV: OR INJECTION
Adults.Loading: 4 g diluted in 250 ml compatible solution and infused over 30 min. Maintenance: 1 to 2 g/hr by continuous infusion.

IM

Adults. 4 to 5 g every 4 hr, p.r.n. Children.20 to 40 mg/kg, repeated p.r.n. To relieve indigestion with hyperacidity

ORALL

(MAGNESIUM HYDROXIDE) Adults and adolescents. 400 to 1,200 mg (5 to 15 ml liquid or 2.5 to 7.5 ml liquid concentrate) up to 4 times daily with water, or 622 to 1,244 mg (tablets or chewable tablets) up to 4 times daily. ,(MAGNESIUM OXIDE) Adults and adolescents.140 mg (capsules) t.i.d. or q.i.d. with water or milk, or 400 to 800 mg daily (tablets). To relieve constipation, to evacuate colon for rectal or bowel examination LIQUID, LIQUID Adults and children age 12 and over. 2.4 to 4.8 g (30 to 60 ml) daily as single dose or divided doses. Children ages 6 to 11. 1.2 to 2.4 g (15 to 30 ml)/day as a single dose or in divided doses. Children ages 2 to 5. 0.4 to 1.2 g (5 to 15 ml) daily as single dose or divided doses.

ORALL

(MAGNESIUM CITRATE) Adults and children age 12 and over.11 to 25 g daily as single dose or divided doses. Children ages 6 to 11. 5.5 to 12.5 g daily as single dose or divided doses. Children ages 2 to 5. 2.7 to 6.25 g daily as single dose or divided doses. Adults and children age 12 and over. 10 to 30 g daily as single dose or divided doses.
DOSAGE ADJUSTMENT Dosage limited to 20 g of magnesium sulfate every 48 hr for patients with severe renal impairment. Children ages 6 to 11. 5 to 10 g daily as a single dose or in divided doses. Children ages 2 to 5. 2.5 to 5 g daily as a single dose or in divided doses. , (MAGNESIUM OXIDE)
Adults.2 to 4 g with a full glass of water or milk, usually at bedtime. Route Onset Peak Duration P.O.* 0.5–3 hr Unknown Unknown P.O. 20 min Unknown 20–180 min I.M. 1 hr Unknown 3–4 hr I.V. Immediate Unknown About 30 min

Mechanism of Action

Assists all enzymes involved in phosphate transfer reactions that use adenosine triphosphate (ATP). Magnesium is required for normal function of the ATP-dependent sodium-potassium pump in muscle membranes. It may effectively treat digitalis glycoside–induced arrhythmias because correction of hypomagnesemia improves the sodium-potassium pump’s ability to distribute potassium into intracellular spaces and because magnesium decreases calcium uptake and potassium outflow through myocardial cell membranes. As a laxative, magnesium exerts a hyperosmotic effect in the small intestine. It causes water retention that distends the bowel and causes the duodenum to secrete For laxative effect. For antacid effect. For anticonvulsant effect. cholecystokinin. This substance stimulates fluid secretion and intestinal motility. As an antacid, magnesium reacts with water, converting magnesium oxide to magnesium hydroxide. Magnesium hydroxide rapidly reacts with gastric acid to form water and magnesium chloride, which increases gastric pH. As an anticonvulsant, magnesium depresses the CNS and blocks peripheral neuromuscular impulse transmission by decreasing available acetylcholine.

Incompatibilities

Don’t combine magnesium sulfate with alkali carbonates and bicarbonates, alkali hydroxides, arsenates, calcium, clindamycin phosphate, dobutamine, fat emulsions, heavy metals, hydrocortisone sodium succinate, phosphates, polymyxin B, procaine hydrochloride, salicylates, sodium bicarbonate, strontium, and tartrates.

Contraindications

Hypersensitivity to magnesium salts or any component of magnesium-containing preparations For magnesium chloride: Coma, heart disease, renal impairment For magnesium sulfate: Heart block, MI, preeclampsia 2 hours or less before delivery (I.V. form) For use as laxative: Acute abdominal problem (as indicated by abdominal pain, nausea, or vomiting), diverticulitis, fecal impaction, intestinal obstruction or perforation, colostomy or ileostomy, severe renal impairment, ulcerative colitis

Interactions

amphotericin B, cisplatin, cyclosporine, gentamicin: Possibly magnesium wasting and need for magnesium
DOSAGE ADJUSTMENT anticholinergics: Possibly decreased absorption and therapeutic effects of these calcium salts (I.V.): Possibly neutralization of magnesium sulfate’s effects cellulose sodium phosphate: Possibly binding with magnesium, possibly decreased therapeutic effectiveness of cellulose
CNS depressants: Increased CNS depression digoxin (I.V.): Possibly heart block and conduction changes, especially when calcium salts are also administered digoxin, fluoroquinolones, folic acid, H2receptor blockers, iron preparations, isoniazid, ketoconazole, penicillamine, phenothiazines, phenytoin, phosphates (oral), tetracyclines: Possibly decreased absorption and blood levels of these diuretics (loop or thiazide): Possibly hypomagnesemia edetate sodium, sodium polystyrene sulfonate: Possibly binding with magnesium enteric-coated : Possibly quicker dissolution of these and increased risk of adverse GI reactions etidronate (oral): Decreased etidronate absorption mecamylamine: Possibly prolonged effects of mecamylamine methenamine, streptomycin, sucralfate, tetracyclines, tobramycin (oral), urinary acidifiers: Possibly decreased therapeutic effects of these misoprostol: Increased misoprostol-induced diarrhea neuromuscular blockers: Possibly increased neuromuscular blockade nifedipine: Possibly increased hypotensive effects when taken with magnesium sulfate potassium-sparing diuretics: Increased risk of hypermagnesemia salicylates: Possibly increased excretion and lower blood levels of salicylates sodium polystyrene sulfonate resin: Possibly metabolic alkalosis high glucose intake: Increased urinary excretion of magnesium
alcohol use: Increased urinary excretion of magnesium

Side Efect

CNS: Confusion, decreased reflexes, dizziness, syncope
CV: Arrhythmias, hypotension
GI: Flatulence, vomiting
MS: Muscle cramps
RESP: Dyspnea, respiratory depression or paralysis
SKIN: Diaphoresis
Other: Allergic reaction, hypermagnesemia, injection site pain or irritation (I.M. form), laxative dependence, magnesium toxicity

Cautions

Be aware that magnesium sulfate is the magnesium 615 M elemental form of magnesium. Oral preparations aren’t all equivalent.

Be aware that drug isn’t metabolized. Drug remaining in the GI tract produces watery stool within 30 minutes to 3 hours.

Make sure patient chews chewable tablets thoroughly before swallowing.

Avoid giving other oral within 2 hours of magnesium-containing antacid.

Before giving drug as laxative, shake oral solution, liquid, or liquid concentrate well and give with a large amount of water.
WARNING Observe for and report early evidence of hypermagnesemia: bradycardia, depressed deep tendon reflexes, diplopia, dyspnea, flushing, hypotension, nausea, slurred speech, vomiting, and weakness.
WARNING Be aware that magnesium may precipitate myasthenic crisis by decreasing patient’s sensitivity to acetylcholine.

Frequently assess cardiac status of patient taking that lower heart rate, such as beta blockers, because magnesium may aggravate symptoms of heart block.
WARNING Magnesium chloride for injection contains the preservative benzyl alcohol, which may cause fatal toxic syndrome in neonates and premature infants.

Provide adequate diet, exercise, and fluids for patient being treated for constipation.

Monitor serum electrolyte levels in patients with renal insufficiency because they’re at risk for magnesium toxicity.

Be aware that magnesium salts aren’t intended for long-term use.

PATIENT SAFTY

Advise patient to chew magnesium chewable tablets thoroughly before swallowing then drink a full glass of water. Mention that tablets have a chalky taste.

Instruct patient to take magnesiumcontaining antacid between meals and at bedtime. Urge him not to take other within 2 hours of the antacid.

Tell patient to notify prescriber and avoid using magnesium-containing laxative if he has abdominal pain, nausea, or vomiting.

Instruct patient to refrigerate magnesium citrate solution.

Caution patient about risk of dependence with long-term laxative use.

Teach patient to prevent constipation by increasing dietary fiber and fluid intake and exercising regularly.

Inform patient that magnesium supplements used to replace electrolytes can cause diarrhea.

Category

Chemical class: Hexahydroxy alcohol
Therapeutic class: Antiglaucoma, diagnostic agent, osmotic diuretic, urinary irrigant

Pregnancy category: B

Indications

To reduce intracranial or intraocular pressure
IV: Adults and adolescents.0.25 to 2 g/kg as 15% to 25% solution given over 30 to 60 min. If used before eye surgery, 1.5 to 2 g/kg 60 to 90 min before procedure. Maximum: 6 g/kg daily.
DOSAGE ADJUSTMENT For small or debilitated patients, dosage reduced to 0.5 g/kg. To diagnose oliguria or inadequate renal function
IV: Adults and adolescents.200 mg/kg or 12.5 g as 15% to 20% solution given over 3 to 5 min. Second dose given only if patient fails to excrete 30 to 50 ml of urine in 2 to 3 hr. Drug discontinued if no response after second dose. Or, 100 ml of 20% solution diluted in 180 ml normal saline solution (forming 280 ml of 7.2% solution) and infused at 20 ml/min; followed by measurement of urine output. Maximum: 6 g/kg daily. To prevent oliguria or acute renal failure
IV: Adults and adolescents.50 to 100 g as 5% to 25% solution. Maximum: 6 g/kg daily. To treat oliguria
IV: Adults and adolescents. 50 to 100 g as 15% to 25% solution given over 90 min to several hr. Maximum: 6 g/kg daily. To promote diuresis in drug toxicity
IV: Adults and adolescents.Loading: 25 g. Maintenance: Up to 200 g as 5% to 25% solution given continuously to maintain urine output of 100 to 500 ml/hr with positive fluid balance of 1 to 2 L. Maximum: 6 g/kg daily. To promote diuresis in hemolytic transfusion reaction
IV:
Adults.20 g given over 5 min and repeated if needed. Maximum: 6 g/kg daily. To provide irrigation during transurethral resection of prostate gland IRRIGATION SOLUTION
Adults.2.5% or 5% solution, as needed. Route Onset Peak Duration I.V.* 1–3 hr Unknown Up to 8 hr I.V. 30–60 min Unknown 4–8 hr I.V. In 15 min Unknown 3–8 hr

Mechanism of Action

Elevates plasma osmolality, causing water to flow from tissues, such as brain and eyes, and from CSF, into extracellular fluid, thereby decreasing intracranial and intraocular pressure. As an osmotic diuretic, mannitol increases the osmolarity of glomerular filtrate, which decreases water reabsorption. This leads to increased excretion of water, sodium, chloride, and toxic substances. As an irrigant, mannitol minimizes the hemolytic effects of water used as an irrigant and reduces the movement of hemolyzed blood from the urethra to the systemic circulation, which prevents hemoglobinemia and serious renal complications.

Incompatibilities

Don’t administer mannitol through same I.V. line as blood or blood products.

Contraindications

Active intracranial bleeding (except during craniotomy), anuria, hepatic failure, hypersensitivity to mannitol or its components, pulmonary edema, severe dehydration, severe heart failure, severe pulmonary congestion, severe renal insufficiency

Interactions

digoxin: Increased risk of digitalis toxicity from hypokalemia diuretics: Possibly increased therapeutic effects of mannitol

Side Efect

CNS: Chills, dizziness, fever, headache, seizures
CV: Chest pain, heart failure, hypertension, tachycardia, thrombophlebitis
EENT: Blurred vision, dry mouth, rhinitis
GI: Diarrhea, nausea, thirst, vomiting
GU: Polyuria, urine retention
RESP: Pulmonary edema
SKIN: Extravasation with edema and tissue necrosis, rash, urticaria
Other: Dehydration, hyperkalemia, hypernatremia, hypervolemia, hypokalemia, hyponatremia (dilutional), metabolic acidosis, water intoxication

Cautions

If crystals form in mannitol solution exposed to low temperature, place solution in hot-water bath to redissolve crystals.

Use a 5-micron in-line filter when administering drug solution of 15% or greater.

During I.V. infusion of mannitol, monitor vital signs, central venous pressure, and fluid intake and output every hour. Measure urine output with indwelling urinary catheter, as appropriate.

Check weight and monitor BUN and serum creatinine electrolyte levels daily.

Provide frequent mouth care to relieve thirst and dry mouth.

PATIENT SAFTY

Inform patient that he may experience dry mouth and thirst during mannitol therapy.

Instruct patient to report chest pain, difficulty breathing, or pain at I.V. site.

Category

Chemical class: Dibenzobicyclooctadiene derivative
Therapeutic class: Antidepressant, tricyclic antidepressant

Pregnancy category: B

To produce diuresis. To decrease intraocular pressure. To decrease intracranial pressure.

Indications

To treat mild to moderate depression Adults and adolescents. Initial: 75 mg daily in divided doses for 2 wk. Increased in 25-mg increments as needed and tolerated. Maintenance: 150 to 225 mg daily in divided doses; for prolonged therapy, possibly 75 to 150 mg daily in divided doses. To treat hospitalized patients with severe depression Adults and adolescents. Initial: 100 to 150 mg daily in divided doses, increased as needed and tolerated. Maintenance: 150 to 225 mg daily in divided doses; for prolonged therapy, possibly 75 to 150 mg daily in divided doses.
DOSAGE ADJUSTMENT For patients over age 60, initial dosage reduced to 25 mg daily and then increased by 25 mg/wk up to maintenance dosage of 50 to 75 mg daily in divided doses. Route Onset Peak Duration P.O. 1–3 wk 3–6 wk Unknown

Mechanism of Action

Blocks norepinephrine’s reuptake at adrenergic nerve fibers. Normally, when a nerve impulse reaches an adrenergic nerve fiber, norepinephrine is released from storage sites and metabolized in the nerve or at the synapse. Some norepinephrine reaches receptor sites on target organs and tissues, but most is taken back into the nerve and stored by way of reuptake mechanism. By blocking norepinephrine reuptake, maprotiline increases its level at nerve synapses. Elevated norepinephrine level may improve mood and decrease depression.

Contraindications

Hypersensitivity to maprotiline, mirtazapine, or their components; use within 14 days of MAO inhibitor therapy

Interactions

anticholinergics, antihistamines: Increased atropine-like adverse effects, such as blurred vision, constipation, dizziness, and dry mouth anticonvulsants: Increased risk of CNS depression, possibly lower seizure threshhold and increased risk of seizures bupropion, clozapine, haloperidol, loxapine, molindone, other tricyclic antidepressants, phenothiazines, pimozide, thioxanthenes, trazodone: Possibly increased anticholinergic effects, possibly lowered seizure threshhold and increased risk of seizures
cimetidine: Possibly increased blood maprotiline level clonidine, guanadrel, guanethidine: Possibly decreased antihypertensive effects of these , possibly increased CNS depression (with clonidine)
CNS depressants: Increased risk of CNS depression estrogens, oral contraceptives containing estrogen: Possibly decreased therapeutic effects and increased adverse effects of maprotiline
MAO inhibitors: Increased risk of hyperpyrexia, hypertensive crisis, severe seizures, or death sympathomimetics: Increased risk of arrhythmias, hyperpyrexia, hypertension, or tachycardia thyroid hormones: Increased risk of arrhythmias
alcohol use: Increased risk of CNS depression

Side Efect

CNS: Agitation, dizziness, drowsiness, fatigue, headache, insomnia, seizures, suicidal ideation, tremor, weakness
EENT: Blurred vision, dry mouth, increased intraocular pressure
ENDO: Gynecomastia
GI: Constipation, diarrhea, epigastric distress, increased appetite, nausea, vomiting
GU: Impotence, libido changes, testicular swelling, urinary hesitancy, urine retention
HEME: Agranulocytosis
SKIN: Diaphoresis, photosensitivity, pruritus, rash
Other: Weight loss

Cautions

Give largest dose of maprotiline at bedtime if daytime drowsiness occurs.

Check CBC, as ordered, if fever, sore throat, or other evidence of agranulocytosis develops.

Take seizure precautions according to facility policy.

Watch patient (especially children, adolescents, and young adults) closely for suicidal tendencies, particularly when therapy starts and dosage changes, because depression may worsen temporarily during these times, possibly leading to suicidal ideation.

Expect to taper drug gradually because stopping abruptly may produce withdrawal symptoms.

PATIENT SAFTY

Advise patient to take maprotiline exactly as prescribed. Caution him not to stop drug abruptly because of risk of withdrawal symptoms, including headache, nausea, nightmares, and vertigo.

Inform patient that he may not feel drug’s effects for several weeks.

Suggest that patient take drug with food if adverse GI reactions develop.

Urge patient to report difficulty urinating, excessive drowsiness, fever, or sore throat.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Caution patient to avoid alcohol and other CNS depressants while taking drug.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes and particularly if patient is a child, teenager, or young adult.

Category

Chemical class: Piperazine derivative
Therapeutic class: Antiemetic, antivertigo

Pregnancy category: B

Indications

To prevent and treat vertigo , CHEWABLE , Adults and adolescents. 25 to 100 mg daily, p.r.n., in divided doses. To treat motion sickness ,
Adults.25 to 50 mg 1 hr before travel and then every 24 hr, p.r.n., for duration of trip. Route Onset Peak Duration P.O. 1 hr Unknown 8–24 hr

Mechanism of Action

May inhibit nausea and vomiting by reducing sensitivity of labyrinthine apparatus and blocking cholinergic synapses in the brain’s vomiting center.

Contraindications

Hypersensitivity to meclizine or its components

Interactions

anticholinergics: Possibly potentiated anticholinergic effects apomorphine: Possibly decreased emetic response to apomorphine
CNS depressants: Possibly potentiated CNS depression
alcohol use: Possibly potentiated CNS depression

Side Efect

CNS: Dizziness, drowsiness, euphoria, excitement, fatigue, hallucinations, headache, insomnia, nervousness, restlessness, vertigo
CV: Hypotension, palpitations, tachycardia
EENT: Blurred vision; diplopia; dry mouth, nose, and throat; tinnitus
GI: Abdominal pain, anorexia, constipation, diarrhea, nausea, vomiting
GU: Urinary frequency and hesitancy, urine retention
RESP: Bronchospasm, thickening of respiratory secretions
SKIN: Jaundice, rash, urticaria

Cautions

Use meclizine cautiously in patients with asthma, glaucoma, or prostate gland enlargement.

Be aware that drug may mask signs of brain tumor, intestinal obstruction, or ototoxicity.

PATIENT SAFTY

Explain that meclizine works best for motion sickness when taken before travel.

Instruct patient to chew meclizine chewable tablets thoroughly before swallowing.

Instruct patient to report blurred vision or drowsiness.

Urge patient to avoid alcohol while taking drug.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to have regular eye examinations during long-term therapy.

Category

Chemical class: Fenamate (anthranilic acid) derivative
Therapeutic class: Analgesic, antidysmenorrheal, anti-inflammatory, antirheumatic

Pregnancy category: Not rated

Indications

To relieve pain and inflammation in rheumatoid arthritis and osteoarthritis Adults and adolescents over age 14. 50 to 100 mg every 6 to 8 hr, p.r.n. Maximum: 400 mg/day. To relieve mild to moderate pain Adults and adolescents over age 14. 50 mg every 4 to 6 hr, p.r.n. Increased to 100 mg every 4 to 6 hr, if needed. Maximum: 400 mg daily. To treat hypermenorrhea and primary dysmenorrhea Adults and adolescents over age 14. 100 mg t.i.d. for up to 6 days. Route Onset Peak Duration P.O.* 1 hr 0.5–2 hr 4–6 hr P.O. Few days 2–3 wk Unknown

Mechanism of Action

Blocks cyclooxygenase, the enzyme needed to synthesize prostaglandins, which mediate the inflammatory response and cause local vasodilation, swelling, and pain. By inhibiting prostaglandins, this NSAID reduces inflammatory symptoms. It also relieves pain because prostaglandins promote pain transmission from periphery to spinal cord.

Contraindications

Hypersensitivity to aspirin, iodides, meclofenamate, other NSAIDs, or their components

Interactions

acetaminophen: Increased risk of adverse renal effects with long-term use of both anticoagulants, thrombolytics: Prolonged PT and increased risk of bleeding antihypertensives: Decreased effectiveness of antihypertensives
beta blockers: Impaired antihypertensive effect of beta blockers cefamandole, cefoperazone, cefotetan, plicamycin,
valproic acid: Hypoprothrombinemia and increased risk of bleeding
cimetidine: Altered meclofenamate level colchicine, glucocorticoids, potassium supplements: Increased GI irritability and bleeding cyclosporine, gold compounds, nephrotoxic : Increased risk of nephrotoxicity digoxin: Increased blood digoxin level insulin, oral antidiabetic : Decreased effectiveness of these lithium: Increased risk of lithium toxicity loop diuretics: Decreased effects of these methotrexate: Increased risk of methotrexate toxicity NSAIDs, salicylates: Increased GI irritability and risk of bleeding, decreased meclofenamate effectiveness
phenytoin: Increased blood phenytoin level probenecid: Increased risk of meclofenamate toxicity
alcohol use: Increased GI irritability and bleeding

Side Efect

CNS: Dizziness, drowsiness, fatigue, headache, insomnia, seizures, stroke
CV: Hypertension, MI, peripheral edema, tachycardia
EENT: Stomatitis, tinnitus
GI: Abdominal pain; anorexia; constipation; diarrhea; diverticulitis; dyspepsia; dysphagia; elevated liver function test results; esophagitis; flatulence; gastritis; gastroenmeclofenamate sodium 620 * For analgesic effect. For antirheumatic effect. teritis; gastroesophageal reflux disease; GI bleeding, perforation, and ulceration; hepatic failure; indigestion; jaundice; melena; nausea; perforation of stomach or intestines; stomatitis; vomiting
GU: Acute renal failure, dysuria, elevated BUN and serum creatinine levels
HEME: Agranulocytosis, anemia, easy bruising, hemolytic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia
RESP: Asthma, respiratory depression
SKIN: Erythema multiforme, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema

Cautions

Use meclofenamate with extreme caution in patients with a history of ulcer disease or GI bleeding because NSAIDs such as meclofenamate increase risk of GI bleeding and ulceration. Expect to use drug for shortest time possible in these patients.

Be aware that serious GI tract ulceration, bleeding, and perforation may occur without
WARNING symptoms. Elderly patients are at greater risk. To minimize risk, give drug with food and a full glass of water. If GI distress occurs, withhold drug and notify prescriber immediately.

Use meclofenamate cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.
WARNING Monitor patient closely for thrombotic events, including MI and stroke, because NSAIDs increase the risk.

Monitor patient—especially if he’s elderly or taking meclofenamate long-term—for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results because, rarely, elevations may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in elderly patients, patients taking diuretics or ACE inhibitors, and patients with heart failure, impaired renal function, or hepatic dysfunction; drug may cause renal failure.

Monitor CBC for decreased hemoglobin and hematocrit because drug may worsen anemia.
WARNING If patient has bone marrow suppression or is receiving an antineoplastic drug, monitor laboratory results (including WBC count), and watch for evidence of infection because anti-inflammatory and antipyretic actions of meclofenamate may mask signs and symptoms, such as fever and pain.

Assess patient’s skin regularly for rash or other hypersensitivity reaction because meclofenamate is an NSAID and may cause serious skin reactions without warning, even in patients with no history of NSAID sensitivity. At first sign of reaction, stop drug and notify prescriber.

Expect lower doses of meclofenamate to be used for long-term therapy.

PATIENT SAFTY

Tell patient to take drug with a full glass of water to keep it from lodging in esophagus and causing irritation. Suggest taking drug with food or milk to avoid GI distress.

Instruct patient to report itching, rash, severe diarrhea, and swelling in ankles or fingers.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Caution pregnant patient not to take NSAIDs such as meclofenamate during last trimester because they may cause premature closure of fetal ductus arteriosus.

Explain that meclofenamate may increase risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, or slurring of speech.

Explain that meclofenamate may increase risk of serious adverse GI reactions; stress importance of seeking immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.

Alert patient to rare but serious skin reactions to meclofenamate. Urge him to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity.

Category

Chemical class: Oxicam derivative
Therapeutic class: Anti-inflammatory

Pregnancy category: C

Indications

To relieve signs and symptoms of osteoarthritis and rheumatoid arthritis ORAL SUSPENSION,
Adults. 7.5 mg daily. Maximum: 15 mg daily. To relieve pauciarticular or polyarticular signs and symptoms of juvenile rheumatoid arthritis ORAL SUSPENSION, Children age 2 and over. 0.125 mg/kg daily. Maximum: 7.5 mg daily.

Mechanism of Action

Blocks cyclooxygenase, the enzyme needed to synthesize prostaglandins, which mediate the inflammatory response and cause local vasodilation, swelling, and pain. By inhibiting prostaglandins, the NSAID meloxicam reduces inflammatory symptoms. It also relieves pain because prostaglandins promote pain transmission from the periphery to the spinal cord.

Contraindications

Angioedema, asthma, bronchospasm, nasal polyps, rhinitis, or urticaria induced by hypersensitivity to aspirin, meloxicam, other NSAIDs, or their components

Interactions

ACE inhibitors: Decreased antihypertensive effect, increased risk of renal failure aspirin: Increased risk of GI ulceration furosemide: Decreased diuretic effect of furosemide, possibly renal impairment lithium: Elevated blood lithium level, possibly lithium toxicity oral anticoagulants,
warfarin: Increased risk of bleeding alcohol use, smoking: Increased risk of GI bleeding

Side Efect

CNS: Confusion, dizziness, fever, headache, insomnia, mood alteration, seizures, stroke
CV: Chest pain, edema, heart failure, hypertension, MI, tachycardia, vasculitis
EENT: Laryngitis, pharyngitis, sinusitis
GI: Abdominal pain, anorexia, colitis, constipation, diarrhea, diverticulitis, dyspepsia, dysphagia, elevated liver function test results, esophagitis, flatulence, gastritis, gastroenteritis, gastroesophageal reflux disease, GI bleeding and ulceration, hepatic failure, hepatitis, indigestion, melena, nausea, pancreatitis, perforation of stomach or intestines, stomatitis, vomiting
GU: Acute renal failure, acute urine retention (children), urinary frequency, UTI
HEME: Agranulocytosis, anemia, easy bruising, hemolytic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia
MS: Arthralgia; back pain; joint crepitation, effusion, or swelling; muscle spasms; myalgia
RESP: Asthma, bronchospasm, cough, dyspnea, respiratory depression, upper respiratory tract infection
SKIN: Erythema multiforme, exfoliative dermatitis, photosensitivity, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, angioedema, flulike symptoms

Cautions

Use meloxicam with extreme caution in patients with history of ulcer disease or GI bleeding because NSAIDs such as meloxicam increase risk of GI bleeding and ulceration. Expect to use drug for shortest time possible in these patients.

Be aware that serious GI tract ulceration, bleeding, and perforation may occur without
WARNING symptoms. Elderly patients are at greater risk. To minimize risk, give drug with food and a full glass of water. If GI distress occurs, withhold drug and notify prescriber immediately.

Use meloxicam cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.
WARNING Monitor patient closely for thrombotic events, including MI and stroke, because NSAIDs increase the risk.

Monitor patient—especially if elderly or taking meloxicam long-term—for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results because, rarely, elevations may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in elderly patients; patients taking diuretics, angiotensin II receptor antagonists, or ACE inhibitors; and patients with heart failure, impaired renal function, or hepatic dysfunction; drug may cause renal failure.

Monitor CBC for decreased hemoglobin and hematocrit. Drug may worsen anemia.
WARNING If patient has bone marrow suppression or is receiving an antineoplastic drug, monitor laboratory results (including WBC count), and watch for evidence of infection because anti-inflammatory and antipyretic actions of meloxicam may mask signs and symptoms, such as fever and pain.

Assess patient’s skin regularly for rash or other hypersensitivity reaction because meloxicam is an NSAID and may cause serious skin reactions without
WARNING, even in patients with no history of NSAID sensitivity. At first sign of reaction, stop drug and notify prescriber.

Monitor patient for adequate hydration before beginning meloxicam therapy to decrease risk of renal dysfunction.

PATIENT SAFTY

Instruct patient to take meloxicam with food or after meals if he has stomach upset.

For oral suspension, tell patient to shake container gently before use.

Caution patient to avoid using other NSAIDs, aspirin, or products containing aspirin while taking meloxicam.

Advise patient to refrain from smoking and alcohol use because these activities may increase risk of adverse GI reactions.

Instruct patient to notify prescriber if he develops signs or symptoms of hepatic dysfunction, such as dark yellow or brown urine, fatigue, fever, itching, lethargy, nausea, or yellowing of eyes or skin.

Advise patient, especially if he’s taking an oral anticoagulant such as warfarin, to report immediately signs of bleeding, such as easy bruising, stomach pain, blood in urine, or black tarry stools.

Caution pregnant patient not to take NSAIDs such as meloxicam during the last trimester because they may cause premature closure of ductus arteriosus.

Explain that meloxicam may increase risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.

Explain that meloxicam may increase risk of serious adverse GI reactions; stress importance of seeking immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.

Alert patient to rare but serious skin reactions. Urge him to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity.

Category

Chemical class: N-methyl-D-aspartate (NMDA) receptor antagonist
Therapeutic class: Antidementia agent

Pregnancy category: B

Indications

To treat moderate-to-severe dementia of the Alzheimer’s type
Adults.Initial: 5 mg daily P.O., increased by 5 mg/wk, as needed, to 10 mg daily in two divided doses; then 15 mg daily with one 5mg and one 10-mg dose daily; then 20 mg daily in two divided doses. Maintenance: 20 mg daily.
DOSAGE ADJUSTMENT Dosage reduction probable for patients with renal impairment.

Contraindications

Hypersensitivity to memantine, amantadine, or their components

Interactions

amantadine, dextromethorphan, ketamine: Possibly additive effects carbonic anhydrase inhibitors, sodium bicarbonate: Decreased memantine clearance, leading to increased blood drug levels and risk of adverse effects cimetidine, hydrochlorothiazide, metformin, nicotinic acid, quinidine, ranitidine, triamterene: Possibly increased blood levels of both agents

Side Efect

CNS: Abnormal gait, agitation, akathisia, anxiety, confusion, delirium, delusions, depression, dizziness, drowsiness, dyskinesia, fatigue, hallucinations, headache, hyperexcitability, insomnia, neuroleptic malignant syndrome, psychosis, restlessness, seizures, somnolence, stroke, tardive dyskinesia
CV: AV block, chest pain, hypertension, peripheral edema, prolonged QT interval, supraventricular tachycardia, tachycardia
ENDO: Hypoglycemia
GI: Acute pancreatitis, anorexia, colitis, constipation, diarrhea, hepatic failure, ileus, nausea, vomiting
GU: Acute renal failure, impotence, urinary incontinence, UTI
HEME: Thrombocytopenia
MS: Arthralgia, back pain
RESP: Bronchitis, cough, dyspnea, upper respiratory tract infection
SKIN: Stevens-Johnson syndrome
Other: Generalized pain, flulike symptoms Memantine blocks the excitatory amino acid glutamate on N-methyl-D-aspartate (NMDA) receptor cells in the CNS. In Alzheimer’s disease, glutamate levels are abnormally high when brain cells are both at rest and active. Normally, when certain brain cells are resting, magnesium ions block NMDA receptors and prevent influx of sodium and calcium ions and outflow of potassium ions. When learning and memory cells in the brain are active, glutamate engages with NMDA receptors, magnesium ions are removed from NMDA receptors, and cells are depolarized. During depolarization, sodium and calcium ions enter brain cells, and potassium ions leave. In Alzheimer’s disease, excessive circulating glutamate permanently removes magnesium ions and opens ion channels. Excessive influx of calcium may damage brain cells and play a major role in Alzheimer’s disease. What’s more, dying brain cells release additional glutamate, worsening the cycle of brain cell destruction. Memantine replaces magnesium on NMDA receptors of brain cells, closing ion channels and preventing calcium influx and the resulting damage to brain cells. By preventing excessive brain cell death, memantine slows progression of Alzheimer’s disease. Mg++ Cell exterior Cell interior Cell membrane Closed ion channel NMDA receptor Memantine Glutamate Glutamate Ca++ Ca++ Na+ K+ K+

Mechanism of Action

Cautions

Use memantine cautionly in patients with renal tubular acidosis or severe UTI because these conditions make urine alkaline, reducing memantine excretion and increasing the risk of

Side Efect

.

Use cautiously in patients with severe hepatic impairment because drug undergoes partial hepatic metabolism, which may increase risk of

Side Efect

.

Monitor patient’s response to memantine, and notify prescriber if serious or bothersome

Side Efect

occur.

PATIENT SAFTY

Advise patient to avoid a diet excessively high in fruits and vegetables because these contribute to alkaline urine, which can alter memantine clearance and increase

Side Efect

.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Category

Chemical class: Phenylpiperidine derivative opioid
Therapeutic class: Analgesic

Pregnancy category: C

Controlled substance schedule: II

Indications

To relieve moderate to severe pain SYRUP,,I.M.OR SUBCUTANEOUS INJECTION
Adults.50 to 150 mg every 3 to 4 hr, p.r.n. Children.1.1 to 1.8 mg/kg every 3 to 4 hr, p.r.n. To provide preoperative sedation
I.V.INJECTION
Adults.15 to 35 mg/hr, p.r.n. I.M. OR SUBCUTANEOUS INJECTION
Adults. 50 to 100 mg 30 to 90 min before surgery. Children. 1 to 2 mg/kg 30 to 90 min before surgery. Maximum: 100 mg every 3 to 4 hr. As adjunct to anesthesia
IV: OR INJECTION
Adults. Individualized. Repeated slow injections of 10 mg/ml solution or continuous infusion of dilute solution (1 mg/ml) titrated as needed. To provide obstetric analgesia I.M. OR SUBCUTANEOUS INJECTION
Adults.50 to 100 mg given with regular, painful contractions; repeated every 1 to 3 hr.
DOSAGE ADJUSTMENT For patients with creatinine clearance of 10 to 50 ml/min/ 1.73 m2, 75% of usual dose is used; with creatinine clearance of less than 10 ml/min/ 1.73 m2, 50% of usual dose is used. Route Onset Peak Duration P.O. 15 min 1–1.5 hr 2–4 hr I.V. 1 min 5–7 min 2–4 hr I.M., 10–15 30–50 2–4 hr SubQ min min

Mechanism of Action

Binds with opiate receptors in the spinal cord and higher levels of the CNS. In this way, meperidine stimulates mu and kappa receptors, which alters the perception of and emotional response to pain.

Incompatibilities

Don’t mix meperidine in same syringe with aminophylline, barbiturates, heparin, iodides, methicillin, morphine sulfate, phenytoin, sodium bicarbonate, sulfadiazine, or sulfisoxazole.

Contraindications

Acute asthma; hypersensitivity to meperidine, opioids, or their components; increased intracranial pressure; severe respiratory depression; upper respiratory tract obstruction; use within 14 days of MAO inhibitor therapy

Interactions

acyclovir, ritonavir: Possibly increased blood meperidine level alfentanil, CNS depressants, fentanyl, sufentanil: Increased risk of CNS and respiratory depression and hypotension amphetamines,
MAO inhibitors: Risk of increased CNS excitation or depression with possibly fatal reactions anticholinergics: Increased risk of severe constipation antidiarrheals (such as loperamide and difenoxin and atropine): Increased risk of severe constipation and increased CNS depression antihypertensives: Increased risk of hypotension buprenorphine: Possibly decreased therapeutic effects of meperidine and increased risk of respiratory depression
cimetidine: Reduced clearance and volume of distribution of meperidine hydroxyzine: Increased risk of CNS depression and hypotension metoclopramide: Possibly decreased effects of metoclopramide naloxone,
naltrexone: Decreased pharmacologic effects of meperidine neuromuscular blockers: Increased risk of prolonged respiratory and CNS depression oral anticoagulants: Possibly increased anticoagulant effect and risk of bleeding
phenytoin: Possibly enhanced hepatic metabolism of meperidine
alcohol use: Possibly increased CNS and respiratory depression and hypotension

Side Efect

CNS: Confusion, depression, dizziness, drowsiness, euphoria, headache, increased intracranial pressure, lack of coordination, malaise, nervousness, nightmares, restlessness, seizures, syncope, tremor
CV: Hypotension, orthostatic hypotension, tachycardia
EENT: Blurred vision, diplopia, dry mouth
GI: Abdominal cramps or pain, anorexia, constipation, ileus, nausea, vomiting
GU: Dysuria, urinary frequency, urine retention
RESP: Dyspnea, respiratory arrest or depression, wheezing
SKIN: Diaphoresis, flushing, pruritus, rash, urticaria
Other: Anaphylaxis, injection site pain, redness, and swelling; physical and psychological dependence

Cautions

Use meperidine with extreme caution in patients with acute abdominal conditions, hepatic or renal disorders, hypothyroidism, prostatic hyperplasia, seizures, or supraventricular tachycardia.

To minimize local anesthetic effect, dilute meperidine syrup with water before use.

Give I.V. dose slowly by direct injection or as a slow continuous infusion. Mix with D5W, normal saline solution, or Ringer’s or lactated Ringer’s solution.

Keep naloxone available when giving I.V. meperidine.

Be aware that subcutaneous injection is painful and isn’t recommended.

Be aware that oral form of meperidine is less than half as effective as parenteral meperidine. Give I.M. form when possible, and expect to increase dosage when switching patient to oral form.

Monitor patient’s respiratory and cardiovascular status during treatment. Notify prescriber immediately and expect to discontinue drug if respiratory rate falls to less than 12 breaths/minute or if respiratory depth decreases.

Monitor patient’s bowel function to detect constipation, and assess the need for stool softeners.

Assess for signs of physical dependence and abuse.

Expect withdrawal symptoms to occur if drug is abruptly withdrawn after longterm use.

PATIENT SAFTY

Inform patient that meperidine is a controlled substance and that he’ll need identification to purchase it.

Advise patient to take drug exactly as prescribed.

Instruct patient to report constipation, severe nausea, and shortness or breath.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to prevent postoperative atelectasis by turning, coughing, and deepbreathing.

Urge patient to avoid alcohol, sedatives, and tranquilizers during therapy.

Category

Chemical class: Sympathomimetic amine
Therapeutic class: Vasopressor

Pregnancy category: C

Indications

To treat hypotension secondary to spinal anesthesia
I.V.INJECTION
Adults.30 to 45 mg (15 mg for obstetric patients); may be repeated, as needed, to maintain blood pressure.
IV:
Adults. Dosage individualized based on patient response to therapy. Average dose is 1 to 5 mg/min. Route Onset Peak Duration I.V. Almost Unknown 15–30 min immediate

Mechanism of Action

Stimulates alpha-adrenergic receptors directly and indirectly, resulting in positive inotropic and chronotropic effects. Indirect stimulation occurs by release of norepinephrine from its storage sites in the heart and other tissues. By enhancing cardiac contraction, mephentermine improves cardiac output, thereby increasing blood pressure. Increased peripheral resistance from peripheral vasoconstriction may also contribute to increased blood pressure. Drug can affect heart rate but change is variable, based on vagal tone. It also may stimulate beta-adrenergic receptors.

Contraindications

Hypersensitivity to mephentermine, phenothiazine-induced hypotension, use within 14 days of MAO inhibitor therapy

Interactions

alpha blockers and other with alphablocking effects: Possibly decreased peripheral vasoconstrictive and hypertensive effects of mephentermine beta blockers (ophthalmic): Decreased effects of mephentermine; increased risk of bronchospasm, wheezing, decreased pulmonary function, and respiratory failure beta blockers (systemic): Increased risk of bronchospasm and decreased effects of both diuretics and other antihypertensives: Possibly reduced effectiveness of these doxapram: Possibly increased vasopressor effects of either drug ergot alkaloids: Increased vasopressor effects guanadrel, guanethidine, mecamylamine, methyldopa, reserpine: Possibly decreased effects of these and increased risk of adverse effects hydrocarbon inhalation anesthetics: Increased risk of atrial and ventricular arrhythmias
MAO inhibitors: Increased, lengthened cardiac stimulation and vasopressor effects, and possibly severe headache and hypertensive crisis maprotiline, tricyclic antidepressants: Increased vasopressor response; increased risk of prolonged QTc interval, arrhythmias, hypertension, and hyperpyrexia
methylphenidate: Possibly increased vasopressor effect of mephentermine nitrates: Possibly reduced antianginal effects of nitrates and decreased vasopressor effect other sympathomimetics (such as dopamine): Possibly increased cardiac effects and

Side Efect

oxytocin: Possibly severe hypertension thyroid hormones: Increased effects of both , increased risk of coronary insufficiency in patients with coronary artery disease

Side Efect

CNS: Anxiety, dizziness, drowsiness, euphoria, headache, incoherence, nervousness, psychosis, restlessness, seizures, weakness
CV: Angina, arrhythmias (including bradycardia, tachycardia, and ventricular arrhythmias), hypertension, hypotension, palpitations, peripheral vasoconstriction
GI: Nausea, vomiting
RESP: Dyspnea
SKIN: Peripheral necrosis

Cautions

Before giving mephentermine, expect to intervene, as ordered, to correct hemorrhage, hypovolemia, metabolic acidosis, or hypoxia.

Discard vial if you observe discoloration or precipitate.

Using D5W or normal saline solution, prepare a 1-mg/ml solution for infusion.

Administer drug using an infusion pump to provide a controlled rate.

Monitor blood pressure, cardiac rate and rhythm, central venous pressure (if appropriate), and urine output during administration. Adjust infusion rate according to patient response, as ordered. Be aware that patients with a history of cardiovascular disease (including hypertension) or hyperthyroidism and chronically ill patients are at increased risk for mephentermine’s adverse cardiovascular effects.

Assess patients with angle-closure glaucoma for signs of an exacerbation, such as eye pain or blurred vision.

Assess circulation in patients with a history of occlusive vascular disease, such as atherosclerosis and Raynaud’s disease, because mephentermine may cause decreased circulation and increase risk of necrosis or gangrene. Inspect I.V. site periodically for signs of extravasation.
WARNING Be aware that weeping, excitability, seizures, and hallucinations are some of the symptoms of mephentermine overdose. Contact prescriber immediately if patient has such symptoms, and expect to provide supportive treatment.

Be aware that mephentermine can increase contractions in pregnant women, especially during third trimester. Expect drug to be prescribed only when benefits outweigh potential adverse effects.

Store drug at 59° to 86° F (15° to 30° C); don’t freeze.

PATIENT SAFTY

Instruct patient receiving mephentermine to report

Side Efect

, including chest pain, difficulty breathing, dizziness, irregular heartbeat, headache, and weakness.

Category

Chemical class: Hydantoin derivative
Therapeutic class: Anticonvulsant

Pregnancy category: Not rated

Indications

To control generalized tonic-clonic, focal, and jacksonian seizures when other are ineffective
Adults. Initial: 50 to 100 mg daily during first wk. Increased by 50 to 100 mg at 1-wk intervals until desired response is reached. Maintenance: 200 to 600 mg daily in equally divided doses. Maximum: 1.2 g daily. Children.Initial: 20 to 50 mg daily. Increased by 25 to 50 mg at 1-wk intervals until desired response occurs. Maintenance: 100 to 400 mg daily in equally divided doses. Maximum: 400 mg daily. To replace other anticonvulsants
Adults. 50 to 100 mg daily during first wk. Dosage gradually increased while decreasing dosage of other drug over 3 to 6 wk. Route Onset Peak Duration P.O. 30 min Unknown 24–48 hr

Mechanism of Action

Limits spread of seizure activity and start of new seizures by:

regulating voltage-dependent sodium and calcium channels in neurons

inhibiting calcium movement across neuronal membranes

enhancing sodium-potassium adenosine triphosphatase activity in neurons and glial cells. These actions may reflect a slowed recovery rate of inactivated sodium channels.

Contraindications

Hypersensitivity to mephenytoin, phenytoin, other hydantoins, or their components

Interactions

acetaminophen: Increased risk of hepatotoxicity with long-term acetaminophen use amiodarone: Possibly increased blood mephenytoin level and risk of toxicity antacids: Possibly decreased mephenytoin effectiveness antineoplastics: Increased mephenytoin metabolism bupropion, clozapine, loxapine, MAO inhibitors, maprotiline, phenothiazines, pimozide,
thioxanthenes: Possibly lowered seizure threshold and decreased therapeutic effects of mephenytoin, possibly intensified CNS depressant effects of these calcium channel blockers, fluconazole, itraconazole, ketoconazole, miconazole, omeprazole: Possibly increased phenytoin level carbamazepine: Decreased blood carbamazepine level, possibly increased blood phenmephenytoin 628 ytoin level and risk of toxicity chloramphenicol, cimetidine, disulfiram, isoniazid, methylphenidate, metronidazole, phenylbutazone, ranitidine, salicylates, sulfonamides, trimethoprim: Possibly impaired metabolism of these and increased risk of mephenytoin toxicity corticosteroids, cyclosporine, digoxin, disopyramide, doxycycline, furosemide, levodopa, mexiletine,
quinidine: Decreased therapeutic effects of these diazoxide: Possibly decreased therapeutic effects of both estrogens, progestins: Decreased therapeutic effects of these , increased blood phenytoin level felbamate: Possibly impaired metabolism and increased blood level of phenytoin fluoxetine: Possibly increased blood phenytoin level and risk of toxicity folic acid: Increased mephenytoin metabolism, decreased seizure control
haloperidol: Possibly lowered seizure threshold and decreased therapeutic effects of mephenytoin; possibly decreased blood haloperidol level insulin, oral antidiabetic : Possibly increased blood glucose level and decreased therapeutic effects of these lamotrigine: Possibly decreased therapeutic effects of lamotrigine lithium: Increased risk of lithium toxicity methadone: Possibly increased methadone metabolism and withdrawal symptoms molindone: Possibly lowered seizure threshold, impaired absorption, and decreased therapeutic effects of mephenytoin oral anticoagulants: Possibly impaired metabolism of these and increased risk of mephenytoin toxicity; possibly increased anticoagulant effect initially, but decreased effect with prolonged therapy oral contraceptives containing estrogen and progestin: Possibly breakthrough bleeding and decreased contraceptive effectiveness
rifampin: Possibly decreased therapeutic effects of mephenytoin streptozocin: Possibly decreased therapeutic effects of streptozocin sucralfate: Possibly decreased mephenytoin absorption tricyclic antidepressants: Possibly lowered seizure threshold and decreased therapeutic effects of mephenytoin; possibly decreased blood level of tricyclic antidepressants
valproic acid: Decreased blood phenytoin level, increased blood valproic acid level vitamin D analogues: Decreased vitamin D analogue activity, risk of anticonvulsantinduced rickets and osteomalacia xanthines: Possibly inhibited mephenytoin absorption and increased clearance of xanthines zaleplon: Increased clearance and decreased effectiveness of zaleplon
alcohol use: Possibly decreased mephenytoin effectiveness

Side Efect

CNS: Ataxia, choreoathetoid movements, confusion, dizziness, drowsiness, excitement, fatigue, fever, headache, peripheral neuropathy, sedation, slurred speech, stuttering, tremor
EENT: Gingival hyperplasia, nystagmus
GI: Constipation, diarrhea, nausea, vomiting
HEME: Agranulocytosis, leukopenia, thrombocytopenia
MS: Muscle twitching
SKIN: Rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Lymphadenopathy, systemic lupus erythematosus

Cautions

Because of mephenytoin’s potentially dangerous adverse effects, expect to use it only when other are ineffective.

Keep in mind that mephenytoin doesn’t control absence seizures.
WARNING Be aware that drug shouldn’t be discontinued abruptly because doing so may cause status epilepticus. Plan to reduce dosage gradually or substitute another drug, as prescribed.

Obtain CBC and differential before treatment, after 2 weeks, and then monthly during first year of treatment, as ordered.

If patient has depressed blood counts, enlarged lymph nodes, or rash, notify prescriber immediately and expect to stop mephenytoin and substitute another drug.

PATIENT SAFTY

Urge patient to take mephenytoin exactly as prescribed and not to stop abruptly.

Advise patient to take drug with food to enhance absorption and reduce adverse GI reactions.

Caution patient on once-a-day therapy to be especially careful not to miss a dose.

Advise patient to report impaired coordination, persistent headache, rash, severe GI distress, swollen gums or lymph nodes, or unusual bleeding or bruising.

Encourage patient to maintain good oral hygiene and to have regular dental checkups to reduce risk of gum disease.

Instruct patient to keep medical appointments to monitor drug effectiveness and check for

Side Efect

. Explain the need for periodic laboratory tests.

Advise patient to wear medical identification stating that he has epilepsy and takes mephenytoin to prevent seizures.

Category

Chemical class: Barbiturate derivative
Therapeutic class: Anticonvulsant, sedative

Pregnancy category: D

Controlled substance schedule: IV

Indications

To treat seizures
Adults.400 to 600 mg daily as a single dose or in divided doses, usually beginning with low dose and increasing over 4 to 5 days until optimum dosage is determined. Children over age 5. 32 to 64 mg t.i.d. or q.i.d. Children under age 5. 16 to 32 mg t.i.d. or q.i.d. To provide sedation
Adults.32 to 100 mg t.i.d. or q.i.d. Children.16 to 32 mg t.i.d. or q.i.d. Route Onset Peak Duration P.O. 30–60 min Unknown 10–16 hr

Mechanism of Action

May reduce seizure activity by reducing transmission of monosynaptic and polysynaptic nerve impulses, which decreases excitability in nerve cells. As a sedative, mephobarbital inhibits upward conduction of nerve impulses to the reticular formation of the brain, which disrupts impulse transmission to the cortex. As a result, mephobarbital depresses the CNS and produces drowsiness, hypnosis, and sedation.

Contraindications

Hepatic disease or failure; history of addiction to sedatives or hypnotics; hypersensitivity to mephobarbital, other barbiturates, or their components; nephritis; porphyria; severe respiratory disease with obstruction or dyspnea

Interactions

acetaminophen: Possibly decreased effects of acetaminophen (with long-term mephobarbital use) anesthetics (halogenated hydrocarbon): Increased risk of hepatotoxicity (with longterm mephobarbital use) carbamazepine, chloramphenicol, corticosteroids, cyclosporine, dacarbazine, digoxin, disopyramide, doxycycline, griseofulvin, metronidazole, oral contraceptives, phenylbutazone, quinidine, theophyllines,
vitamin D: Decreased effectiveness of these
CNS depressants: Increased CNS depression divalproex sodium,
valproic acid: Increased risk of CNS depression and neurotoxicity guanadrel, guanethidine: Increased risk of orthostatic hypotension
haloperidol: Possibly decreased blood haloperidol level and change in seizure pattern hydantoins: Possibly interference with hydantoin metabolism leucovorin: Possibly decreased anticonvulsant effect of mephobarbital maprotiline: Possibly increased CNS depression and decreased therapeutic effects of mephobarbital
mexiletine: Possibly decreased blood mexiletine level oral anticoagulants: Possibly decreased therapeutic effects of anticoagulants, possibly increased risk of bleeding when mephobarbital is discontinued tricyclic antidepressants: Possibly decreased therapeutic effects of tricyclic antidepressants
alcohol use: Increased CNS depression

Side Efect

CNS: Agitation, anxiety, ataxia, confusion, delusions, depression, dizziness, drowsiness, fever, hallucinations, headache, insomnia, irritability, nervousness, nightmares, paradoxical stimulation, seizures, syncope, tremor
CV: Orthostatic hypotension
EENT: Vision changes
GI: Anorexia, constipation, hepatic dysfunction, nausea, vomiting
HEME: Agranulocytosis
MS: Arthralgia, bone pain, muscle twitching or weakness
RESP: Respiratory depression
SKIN: Exfoliative dermatitis, rash, StevensJohnson syndrome
Other: Physical and psychological dependence, weight loss

Cautions

Observe patient for signs of physical and psychological dependence, especially with prolonged use at high doses.

Observe for signs of chronic barbiturate intoxication, including confusion, insomnia, poor judgment, slurred speech, and unsteady gait.

Assess for paradoxical stimulation in patient who receives drug for acute or chronic pain.
WARNING Expect to taper mephobarbital gradually when discontinuing. Be aware that withdrawal symptoms can be severe and may cause death. Mild signs and symptoms may include anxiety, muscle twitching, nausea, orthostatic hypotension, and progressive weakness and may appear 8 to 12 hours after last dose. More severe signs include delirium and seizures.

PATIENT SAFTY

Advise patient to take mephobarbital exactly as prescribed. Caution him not to stop taking drug abruptly because of possible withdrawal symptoms and, for epileptic patients, seizures.

Instruct patient to avoid alcohol, sleeping pills, and other sedatives while taking mephobarbital because of the risk of increased CNS depression.

Advise patient to avoid hazardous activities until CNS effects of drug are known.

Advise patient to change position slowly to minimize orthostatic hypotension.

Urge patient to report confusion, fever, rash, or severe dizziness.

Category

Chemical class: Carbamate derivative
Therapeutic class: Antianxiety

Pregnancy category: Not rated

Controlled substance schedule: IV

Indications

To treat anxiety S.R. Adults and adolescents.400 to 800 mg every morning and bedtime. Maximum: 2,400 mg daily. Children ages 6 to 12. 200 mg every morning and bedtime. Adults and adolescents. 1,200 to 1,600 mg/ day in divided doses t.i.d. or q.i.d. Maximum: 2,400 mg daily.
DOSAGE ADJUSTMENT For patients with creatinine clearance of 10 to 50 ml/min/ 1.73 m2, drug given every 12 hr; with creatinine clearance less than 10 ml/min/ 1.73 m2, drug given every 18 hr. Children ages 6 to 12. 200 to 600 mg daily in divided doses b.i.d. or t.i.d. Route Onset Peak Duration P.O. 1 hr Unknown Unknown

Mechanism of Action

May act at multiple sites in CNS, including thalamus and limbic system. Meprobamate inhibits spinal reflexes, causing CNS relaxation; its sedative effects may account for its anticonvulsant action. It also has muscle relaxant properties.

Contraindications

Hypersensitivity to meprobromate or related , such as carisoprodol; porphyria

Interactions

CNS depressants: Increased CNS depression
alcohol use: Increased CNS depression

Side Efect

CNS: Ataxia, dizziness, drowsiness, euphoria, headache, paradoxical stimulation, paresthesia, slurred speech, syncope, vertigo, weakness
CV: Arrhythmias, including tachycardia; hypotension; palpitations
EENT: Impaired visual accommodation
GI: Diarrhea, nausea, vomiting
SKIN: Erythematous maculopapular rash, pruritus, urticaria
Other: Physical dependence

Cautions

Use meprobamate cautiously in patients with impaired hepatic or renal function, seizure disorders, or suicidal tendencies.

Also use drug cautiously in patients with history of drug dependence or abuse because meprobamate use can lead to physical dependence and abuse.

Observe for evidence of chronic drug intoxication, such as ataxia, slurred speech, and vertigo.
WARNING When stopping therapy, expect to taper dosage over 2 weeks because stopping abruptly can worsen previous symptoms, such as anxiety, or cause withdrawal symptoms, such as confusion, hallucinations, muscle twitching, tremor, and vomiting.

PATIENT SAFTY

Instruct patient to take meprobamate exactly as directed and not to stop taking it abruptly.

Advise patient not to crush or chew S.R. capsules.

Instruct patient to avoid hazardous activities until drug’s CNS effects are known.

Direct patient to avoid alcohol, sedatives, and other CNS depressants while taking meprobamate.

Inform patient that drug may become less effective after several months of treatment.

Instruct patient to report rash.

Category

Chemical class: Carbapenem
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat complicated appendicitis and peritonitis caused by susceptible strains of alpha-hemolytic streptococci, Bacteroides fragilis, Bacteroides thetaiotaomicron, Escherichia coli, Klebsiella pneumoniae, Peptostreptococcus species, or Pseudomonas aeruginosa
IV: OR INJECTION Adults and children weighing more than 50 kg (110 lb). 1 g every 8 hr infused over 15 to 30 min or given as a bolus over 3 to 5 min. Children over age 3 months weighing less than 50 kg. 20 mg/kg every 8 hr infused over 15 to 30 min or given as bolus over 3 to 5 min. Maximum: 1 g every 8 hr.
DOSAGE ADJUSTMENT For patients with creatinine clearance of 26 to 50 ml/min/ 1.73 m2, dosage reduced to 1 g every 12 hr. For those with clearance of 10 to 25 ml/ min/1.73 m2, dosage reduced to 500 mg every 12 hr. For those with clearance less than 10 ml/min/1.73 m2, dosage reduced to 500 mg every 24 hr. To treat complicated skin and skin structure infections caused by Staphylococcus aureus, Streptococcus agalactiae, Streptococcus pyogenes, viridans group streptococci, Enterococcus faecalis (excluding vancomycin-resistant isolates), Pseudomonas aeruginosa, Escherichia coli, Proteus mirabilis, Bacteroides fragilis, and Peptostreptococcus species
IV: Adults and children weighing more than 50 kg (110 lb). 500 mg every 8 hr infused over 15 to 30 min. Children over age 3 months weighing less than 50 kg. 10 mg/kg every 8 hr infused over 15 to 30 min. Maximum: 500 mg every 8 hr.
DOSAGE ADJUSTMENT For patients with creatinine clearance of 26 to 50 ml/min/ 1.73 m2, dosage reduced to 500 mg every 12 hr. For those with clearance of 10 to 25 ml/min/1.73 m2, dosage reduced to 250 mg every 12 hr. For those with clearance less than 10 ml/min/1.73 m2, dosage reduced to 250 mg every 24 hr. To treat bacterial meningitis caused by Haemophilus influenzae, Neisseria meningitidis, or Streptococcus pneumoniae in children
IV: OR INJECTION Children weighing more than 50 kg. 2 g every 8 hr infused over 15 to 30 min or given as a bolus over 3 to 5 min. Children over age 3 months weighing less than 50 kg. 40 mg/kg every 8 hr infused over 15 to 30 min or given as bolus over 3 to 5 min. Maximum: 2 g every 8 hr.

Mechanism of Action

Penetrates cell walls of most gramnegative and gram-positive bacteria, inactivating penicillin-binding proteins. This action inhibits bacterial cell wall synthesis and causes cell death.

Incompatibilities

Don’t mix meropenem in same solution with other .

Contraindications

Hypersensitivity to meropenem, other carbapenem , beta lactams, or their components

Interactions

probenecid: Inhibited renal excretion of meropenem
valproic acid: Possibly reduced blood level of valproic acid to subtherapeutic level

Side Efect

CNS: Headache, seizures
CV: Shock
EENT: Epistaxis, glossitis, oral candidiasis
GI: Anorexia, constipation, diarrhea, elevated liver function test results, nausea, pseudomembranous colitis, vomiting
GU: Elevated BUN and serum creatinine levels, hematuria, renal failure
HEME: Agranulocytosis, hemolytic anemia, leukopenia, neutropenia, positive Coombs’ test
RESP: Apnea, dyspnea
SKIN: Diaper rash from candidiasis (children), erythema multiforme, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis; angioedema; injection site inflammation, pain, phlebitis, or thrombophlebitis; sepsis

Cautions

Obtain body fluid and tissue samples, as ordered, for culture and sensitivity testing. Expect to review test results, if possible, before giving first dose of meropenem.

For I.V. bolus, add 10 ml sterile water for injection to 500 mg/20-ml vial, or 20 ml diluent to 1 g/30-ml vial of drug. Shake to dissolve.
WARNING Be aware that fatal hypersensitivity reactions have occurred with meropenem use. Determine whether patient has had previous reactions to antibiotics or other allergens. Monitor patient closely and stop drug immediately if signs and symptoms of anaphylaxis occur. Notify prescriber, and expect to provide supportive emergency care that may include epinephrine and I.V. steroid administration, oxygen, and airway management.

Monitor patient closely for diarrhea, which may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold meropenem and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Take seizure precautions according to facility policy, especially for patients with bacterial meningitis or CNS or renal disorders because of an increased risk of seizures with meropenem.

Monitor patient with creatinine clearance of 10 to 26 ml/min/1.73 m2for signs and symptoms of seizures, heart failure, renal failure, or shock.

PATIENT SAFTY

Tell patient to report trouble breathing, injection site pain, and sore mouth.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and can be serious, requiring prompt treatment.

Category

Chemical class: 5-Aminosalicylic acid derivative
Therapeutic class: Anti-inflammatory

Pregnancy category: B

Indications

To treat and maintain remission of ulcerative colitis DELAYED-RELEASE (ASACOL)
Adults. Initial: 0.8 g t.i.d. for 6 wk. Maintenance: 1.6 g daily in divided doses. DELAYED-RELEASE (MESASAL)
Adults. 1.5 to 3 g daily in divided doses for 6 wk. DELAYED-RELEASE (SALOFALK)
Adults. 1 g t.i.d. or q.i.d. for 6 wk.
Adults. 1 g q.i.d. for up to 8 wk. To treat mild to moderate distal ulcerative colitis, proctitis, and proctosigmoiditis RECTAL SUSPENSION
Adults. 4 g (60 ml) daily at bedtime for 3 to 6 wk. To treat active ulcerative proctitis SUPPOSITORIES(CANASA)
Adults. 0.5 g b.i.d. or t.i.d. for 3 to 6 wk. Or 1 g at bedtime for 3 to 6 wk. To induce remission in patients with active mild to moderate ulcerative colitis.
Adults. 2.4 or 4.8 g once daily with a meal for up to 8 wk.

Mechanism of Action

May reduce inflammation by inhibiting the enzyme cyclooxygenase and decreasing production of arachidonic acid metabolites, which may be increased in patients with inflammatory bowel disease. Cyclooxygenase is needed to form prostaglandins from arachidonic acid. Prostaglandins mediate inflammatory activity and produce signs and symptoms of inflammation. Mesalamine also may reduce inflammation by interfering with leukotriene synthesis and inhibiting the enzyme lipoxygenase, both of which take part in inflammatory response.

Contraindications

Hypersensitivity to mesalamine, salicylates, or their components

Interactions

digoxin: Possibly decreased absorption and bioavailability of digoxin lactulose: Possibly interference with delayed-release tablets or capsules omeprazole: Increased mesalamine absorption

Side Efect

CNS: Chills, confusion, depression, dizziness, emotional lability, fatigue, fever, headache (severe), somnolence, tremor, vertigo, weakness
CV: Myocarditis, pericarditis
EENT: Blurred vision, dry mouth, rhinitis, taste perversion, tinnitus
GI: Abdominal cramps or pain (severe), anorexia, bloody diarrhea, cholecystitis, colitis, diarrhea, elevated liver function test results, flatulence, gastritis, hepatotoxicity, hepatitis, indigestion, nausea, pancreatitis, rectal pain, vomiting
GU: Acute or chronic renal failure, interstitial nephritis, nephrotoxicity
HEME: Agranulocytosis, anemia including aplastic anemia, eosinophilia, granulocytopenia, leukopenia, lymphadenopathy, thrombocytopenia
MS: Back pain, dysarthria, gout
RESP: Allergic alveolitis, asthma exacerbation, fibrosing alveolitis, pleuritis, pneumonitis
SKIN: Acne, alopecia, dryness, erythema nodosum, pruritus, rash, urticaria
Other: Angioedema, drug fever, systemic lupus erythematosus

Cautions

Use mesalamine cautiously in patients with sulfite sensitivity. Some drug formulations contain sulfites, which may cause hypersensitivity reactions in these patients.

Use mesalamine cautiously in patients with liver disease because hepatic dysfunction may occur.

Ensure that suppository is firm before inserting it. If it’s too soft, chill in refrigerator for 30 minutes or run under cold water before removing wrapper. Moisten with water-soluble lubricant or tap water before insertion. Have patient retain suppository for 1 to 3 hours, as directed.

Give rectal suspension at bedtime, and have patient retain for prescribed time— about 8 hours, if possible. Retention time ranges from 3.5 to 12 hours.

Be aware that rectal suspension may darken slightly over time but that this change doesn’t affect potency. Discard rectal suspension that turns dark brown.

Assess patient for evidence of acute intolerance similar to flare-up of inflammatory bowel disease: acute abdominal cramps and pain, bloody diarrhea, and, possibly, fever, headache, and rash.

For patients with impaired renal function, expect to monitor renal function test results periodically during long-term therapy because drug may cause nephrotoxicity.

Monitor patient’s CBC with differential for eosinophilia, which may indicate an allergic reaction.

PATIENT SAFTY

Instruct patient taking oral drug to swallow tablets or capsules whole and not to break outer coating by cutting or chewing.

Tell patient taking extended-release product to take it with a meal.

Teach patient how to use rectal suspension or suppositories correctly. Stress shaking suspension bottle well before using.

Advise patient to notify prescriber immediately about abdominal cramps or pain, bloody diarrhea, fever, headache, or rash.

Category

Chemical class: Alkylpiperidine phenothiazine derivative
Therapeutic class: Antipsychotic

Pregnancy category: Not rated

Indications

To treat schizophrenia in patients who failed to respond to other antipsychotic , either because they were ineffective or because intolerable adverse effects prevented attainment of effective dose

ORALL

, Adults and adolescents. 50 mg t.i.d., increased as needed and tolerated. Maximum: 400 mg daily.

IM

Adults and adolescents. 25 mg, repeated in 30 to 60 min, as needed. Maximum: 200 mg/day. Route Onset Peak Duration P.O., I.M. Up to 6 wk– 4–8 hr several wk 6 mo

Mechanism of Action

Depresses brain areas that control activity and aggression—including cerebral cortex, hypothalamus, and limbic system—by an unknown mechanism.

Contraindications

Blood dyscrasias; bone marrow depression; cerebral arteriosclerosis; coma; concurrent use of high doses of CNS depressants; concurrent use of other that prolong QTc interval, such as disopyramide, procainamide, and quinidine; congenital long-QT syndrome; coronary artery disease; hepatic dysfunction; history of arrhythmias; hypersensitivity to mesoridazine, other phenothiazines, or their components; myeloproliferative disorders; severe CNS depression; severe hypertension or hypotension; subcortical brain damage

Interactions

aluminumor magnesium-containing antacids, antidiarrheals (adsorbent): Decreased mesoridazine absorption amantadine, anticholinergics: Increased anticholinergic effects, possibly decreased therapeutic effects of mesoridazine aminoglycosides, ototoxic : Masked symptoms of ototoxicity, such as dizziness, tinnitus, and vertigo anticonvulsants: Possibly lowered seizure threshold antithyroid : Increased risk of agranulocytosis appetite suppressants: Possibly antagonized anorectic effect astemizole, cisapride, disopyramide, erythromycin, pimozide, probucol, procainamide,
quinidine: Increased risk of prolonged QT interval and life-threatening arrhythmias
beta blockers: Increased blood levels of both , possibly resulting in additive hypotension, retinopathy, arrhythmias, and tardive dyskinesia CNS depressants, general anesthetics: Increased CNS depression dextroamphetamine: Possibly interference with action of either drug levodopa: Possibly inhibited levodopa effects lithium: Possibly decreased absorption of mesoridazine opioid analgesics: Possibly decreased mesoridazine effects; increased CNS and respiratory depression and orthostatic hypotension; increased risk of severe constipation oral anticoagulants: Possibly decreased therapeutic effects of anticoagulants sympathomimetics: Possibly decreased therapeutic effects of these and increased risk of hypotension thiazide diuretics: Possibly orthostatic hypotension, hyponatremia, and water intoxication tricyclic antidepressants: Increased tricyclic antidepressant levels, inhibited mesoridazine metabolism, increased risk of neuroleptic malignant syndrome
alcohol use: Increased CNS depression

Side Efect

CNS: Ataxia, dizziness, drowsiness, extrapyramidal reactions (tardive dyskinesia, pseudoparkinsonism), fever, neuroleptic malignant syndrome, restlessness, seizures, slurred speech, syncope, tremor, weakness
CV: Hypotension, orthostatic hypotension, prolonged QTc interval, torsades de pointes
EENT: Blurred vision, dry mouth, hypertrophic papillae of tongue, increased salivation, photophobia
ENDO: Galactorrhea, gynecomastia
GI: Constipation, hepatotoxicity, nausea, vomiting
GU: Dysuria, ejaculation disorders, impotence, menstrual irregularities, priapism
HEME: Agranulocytosis, leukopenia, thrombocytopenia
SKIN: Contact dermatitis, decreased sweating, jaundice, photosensitivity, rash
Other: Injection site pain, weight gain

Cautions

Before starting mesoridazine, expect to obtain a 12-lead ECG to detect prolonged QTc interval. If patient’s QTc interval is greater than 450 milliseconds (msec), expect to withhold drug because of risk of life-threatening torsades de pointes.

Wear gloves when working with liquid and parenteral forms of mesoridazine, and avoid contact with clothing or skin; drug may cause contact dermatitis.

Discard injection solution if it’s frankly discolored or contains precipitate; slightly yellow color is acceptable.

Inject I.M. drug deep into upper outer quadrant of buttocks; massage area afterward to prevent sterile abscess.

Implement continuous ECG monitoring, as ordered, to detect arrhythmias. Expect to discontinue mesoridazine if the QTc interval exceeds 500 msec.

Monitor serum potassium level before and during therapy, and administer potassium supplements as prescribed.

Assess patient for hypotension and orthostatic hypotension, especially during I.M. use. Notify prescriber if either develops.
WARNING Monitor patient for neuroleptic malignant syndrome, a potentially fatal reaction to antipsychotic , and notify prescriber about such early signs as altered mental status, fever, hypertension or hypotension, muscle rigidity, and tachycardia.

Assess patient for signs of blood dyscrasias, including cellulitis, fever, and pharyngitis. If they develop, expect to stop drug.

Monitor patient for signs of tardive dyskinesia, even after treatment stops. Notify prescriber if they develop.

Expect to taper drug dosage before discontinuation to avoid

Side Efect

, such as dizziness, nausea, tremor, and vomiting.

PATIENT SAFTY

Instruct patient to take drug exactly as prescribed and not to stop abruptly.

Explain that I.M. injection may be painful.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to change position slowly to minimize orthostatic hypotension.

Tell patient to report fever, involuntary facial movements, sore throat, unusual bleeding or bruising, and yellowing of eyes or skin.

Urge patient to avoid alcohol and prolonged sun exposure during therapy.

If patient need long-term therapy, explain the risk of tardive dyskinesia. Also advise him to have regular eye examinations.

Category

Chemical class: Sympathomimetic amine
Therapeutic class: Antiasthmatic, bronchodilator

Pregnancy category: C

Indications

To treat bronchospasm SYRUP, Adults and children age 9 or over weighing more than 27 kg (59 lb). 20 mg every 6 to 8 hr. Children ages 6 to 9 weighing 27 kg or less. 10 mg every 6 to 8 hr. INHALATION AEROSOL Adults and adolescents.2 to 3 inhalations (1.3 to 1.95 mg) every 3 to 4 hr. Maximum: 12 inhalations daily. Children ages 6 to 12. 1 to 3 inhalations (0.65 to 1.95 mg) every 3 to 4 hr. Maximum: 12 inhalations daily. INHALATION NEBULIZER Adults and adolescents. 0.2 to 0.3 ml of 5% solution diluted in 2.5 ml normal saline solution t.i.d. or q.i.d., p.r.n., but no more than every 4 hr. Children ages 6 to 12. 0.1 to 0.2 ml of 5% solution diluted in normal saline solution to a total volume of 3 ml t.i.d. or q.i.d., p.r.n., but no more than every 4 hr. Route Onset Peak Duration P.O. 15 min 1 hr 4 hr or longer Inhalation 1 min 1 hr 4 hr or (aerosol) longer Inhalation 5–30 Unknown 4 hr or (nebulizer) min longer

Mechanism of Action

Attaches to beta2receptors on bronchial cell membranes, which stimulates intracellular enzyme adenyl cyclase to convert adenosine triphosphate to cyclic adenosine monophosphate (cAMP). Increased intracellular cAMP level relaxes bronchial smooth-muscle cells and inhibits histamine release.

Contraindications

Angina, cerebral arteriosclerosis, dilated heart failure, heart block from digitalis toxicity, hypersensitivity to metaproterenol or its components, labor, local anesthesia, organic brain damage, tachyarrhythmias

Interactions

beta blockers: Increased risk of bronchospasm MAO inhibitors, tricyclic antidepressants: Possibly potentiated cardiovascular effects of metaproterenol other sympathomimetics: Possibly additive effects of both and risk of toxicity
theophylline: Increased risk of arrhythmias

Side Efect

CNS: Dizziness, fatigue, headache, insomnia, malaise, nervousness, tremor
CV: ECG changes, hypertension, palpitations, tachycardia
EENT: Dry mouth, pharyngitis, taste perversion
GI: Diarrhea, nausea, vomiting
RESP: Asthma exacerbation, cough

Cautions

Anticipate that a single dose of nebulized metaproterenol may not completely stop an acute asthma attack.

Monitor for

Side Efect

and signs of toxicity, especially if patient uses tablets and aerosol. Notify prescriber if they develop.

Be aware that tolerance may occur with continued use.

PATIENT SAFTY

Caution patient not to use metaproterenol inhaler or nebulizer more often than prescribed.

Teach patient to use metaproterenol inhaler correctly, to hold breath during second half of inhalation, and to wait 2 minutes between inhalations.

Instruct parents to use spacer with their child’s metered-dose inhaler.

Advise patient to use metaproterenol 5 minutes before using corticosteroid inhaler, if prescribed, to maximize airway opening and drug effects.

Instruct patient to immediately report diarrhea, increased shortness of breath, insomnia, or irregular heartbeat.

Instruct patient to notify prescriber if drug becomes less effective.

Category

Chemical class: Oxazolidinone derivative
Therapeutic class: Skeletal muscle relaxant

Pregnancy category: Not rated

Indications

To relieve discomfort caused by acute, painful musculoskeletal conditions Adults and children over age 12. 800 mg t.i.d. or q.i.d. Route Onset Peak Duration P.O. Usually Unknown 4–6 hr in 1 hr

Mechanism of Action

May depress CNS, causing sedation, which in turn may reduce skeletal muscle spasms to provide pain relief. Metaxalone doesn’t directly relax tense skeletal muscles.

Contraindications

Hypersensitivity to metaxalone or its components, significant renal or hepatic disease, tendency to develop drug-induced, hemolytic, or other anemias

Interactions

CNS depressants: Increased CNS depression
alcohol use: Increased CNS depression

Side Efect

CNS: Dizziness, drowsiness, excitement, general CNS depression, headache, insomnia, irritability, nervousness, restlessness
GI: Abdominal cramps or pain, GI upset, jaundice, hepatotoxicity, nausea, vomiting
HEME: Hemolytic anemia, leukopenia
SKIN: Pruritus, rash

Cautions

Metaxalone may not be prescribed for women who are or may become pregnant unless potential benefits outweigh risks because drug’s effect on fetus is unknown.

Expect to avoid giving metaxalone with food because food may increase CNS depression, especially in elderly patients.

Monitor patient for excessive drowsiness, which may lead to respiratory depression.

Caution patient to consult prescriber before taking other , such as sleeping pills, cold or allergy preparations, opioid analgesics, and antidepressants.

Monitor liver function test results for elevations, especially in patients with preexisting hepatic disease.

Monitor renal function test results, as prescribed, for signs of impaired renal function because drug is excreted by kidneys.

Provide rest and other pain-relief measures.

Store drug at 59° to 86° F (15° to 30° C).

PATIENT SAFTY

Advise patient to take metaxalone tablets exactly as prescribed and not to increase dosage or frequency.

Instruct patient to take metaxalone tablets on an empty stomach.

Caution patient to avoid hazardous activities, such as driving or operating machinery, until drug’s CNS effects are known.

Instruct patient to avoid alcohol and other CNS depressants during therapy.

Urge patient to notify prescriber if he notices a rash or itching, which may signify a hypersensitivity reaction, or if he develops signs of hepatotoxicity, such as tiredness, nausea, yellow skin, or flulike symptoms.

Category

Chemical class: Dimethylbiguanide
Therapeutic class: Antidiabetic

Pregnancy category: B

Indications

To reduce blood glucose level in type 2 diabetes mellitus

ORALL

, Adults and children age 10 and over. Initial: 500 mg b.i.d. or 850 mg daily, increased as prescribed by 500 mg/wk or by 850 mg every 2 wk until desired response occurs. Usual: 500 to 850 mg b.i.d. or t.i.d. Maximum: 2,550 mg daily (adults and adolescents age 17 and over); 2,000 mg daily (children ages 10 to 16).
DOSAGE ADJUSTMENT If patient uses insulin, initial dosage reduced to 500 mg daily and then increased as prescribed by 500 mg weekly until blood glucose level is controlled. (GLUCOPHAGE XR, GLUMETZA).Adults and adolescents age 18 and over. Initial: 500 mg daily (Glucophage XR) or 1,000 mg daily (Glumetza) with evening meal. Increased as prescribed by 500 mg/ wk. Maximum: 2,000 mg daily.
DOSAGE ADJUSTMENT If control isn’t achieved with maximum once-daily dosage, regimen may be changed to 1,000 mg b.i.d. If control isn’t achieved after 4 wk of maximum dosage, an oral sulfonylurea may be prescribed. (FORTAMET) Adults and adolescents age 17 and over. Initial: 500 to 1,000 mg once daily in evening. Increased in increments of 500 mg weekly, as needed. Maximum: 2,500 mg daily. If control isn’t achieved after 4 wk at maximum dosage, an oral sulfonylurea may be prescribed. As adjunct to insulin therapy in type 2 diabetes mellitus

ORALL

, ,
Adults.Initial: 500 mg (Glucophage, Glucophage XR, Fortamet) or 1,000 mg (Glumetza) daily in addition to current dose of insulin. Increased by 500 mg/wk, as needed. Maximum: 2,000 mg for Glucophage XR and Glumetza; 2,500 mg for Glucophage and Fortamet.
DOSAGE ADJUSTMENT If fasting blood glucose level drops below 120 mg/dl, insulin dosage decreased by 10% to 25%. Subsequent insulin dosage decrease may be needed based upon patient’s continued response. Route Onset Peak Duration P.O. Unknown Up to 2 wk after (tablets) 2 wk drug discontinued

Mechanism of Action

May promote storage of excess glucose as glycogen in the liver, which reduces glucose production. Metformin also may improve glucose use by skeletal muscle and adipose tissue by increasing glucose transport across cell membranes. This drug also may increase the number of insulin receptors on cell membranes and make them more sensitive to insulin. In addition, metformin modestly decreases blood triglyceride and total cholesterol levels.

Contraindications

Hypersensitivity to metformin or its components, impaired renal function, metabolic acidosis, use of iodinated contrast media within preceding 48 hours

Interactions

calcium channel blockers, corticosteroids, estrogens, isoniazid, nicotinic acid, oral contraceptives, phenothiazines, phenytoin, sympathomimetics, thiazide and other diuretics, thyroid : Possibly hyperglycemia cationic (such as amiloride, cimetidine, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim, vancomycin), nifedipine: Increased blood metformin level clofibrate, MAO inhibitors, probenecid, propranolol, rifabutin, rifampin, salicylates, sulfonamides, sulfonylureas: Increased risk of hypoglycemia all : Possibly delayed metformin absorption
alcohol use: Increased risk of hypoglycemia and lactate formation

Side Efect

CNS: Headache
EENT: Metallic taste
ENDO: Hypoglycemia
GI: Abdominal distention, anorexia, constipation, diarrhea, flatulence, indigestion, nausea, vomiting
HEME: Aplastic anemia, megaloblastic anemia, thrombocytopenia
SKIN: Photosensitivity, rash
Other: Lactic acidosis, weight loss

Cautions

Give metformin tablets with food, which decreases and slightly delays absorption, thus reducing risk of adverse GI reactions. Give tablets with evening meal; don’t break or crush them.

Expect prescriber to alter dosage if patient has a condition that decreases or delays gastric emptying, such as diarrhea, gastroparesis, GI obstruction, ileus, or vomiting.

Expect to assess BUN and serum creatinine level before and during long-term therapy in those at increased risk for lactic acidosis. metformin hydrochloride 639 M

Monitor patient’s hepatic function, as ordered, because impaired hepatic function may significantly reduce the liver’s ability to clear lactate, predisposing the patient to lactic acidosis.

Monitor patient’s blood glucose level to evaluate drug effectiveness. Assess for hyperglycemia and the need for insulin during times of increased stress, such as infection and surgery.

Withhold drug, as ordered, if patient becomes dehydrated or develops hypoxemia or sepsis because these conditions increase the risk of lactic acidosis.

Iodinated contrast media used in radiographic studies increases risk of renal failure and lactic acidosis during metformin therapy. Expect to withhold drug for 48 hours before and after testing.

PATIENT SAFTY

Instruct patient to take metformin tablet at breakfast if taking drug once a day or at breakfast and dinner if taking drug twice a day. Instruct him to take tablets once daily with evening meal and to swallow them whole without crushing or chewing.

Direct patient to take drug exactly as prescribed and not to change the dosage or frequency unless instructed.

Stress importance of following prescribed diet, exercising regularly, controlling weight, and checking blood glucose level.

Teach patient how to measure blood glucose level and recognize hyperglycemia and hypoglycemia. Urge him to notify prescriber of abnormal blood glucose level.

Caution patient to avoid alcohol, which can increase the risk of hypoglycemia.

Instruct patient to report early signs of lactic acidosis, including drowsiness, hyperventilation, malaise, and muscle pain.

Advise patient to expect laboratory testing of glycosylated hemoglobin every 3 months until blood glucose is controlled.

Category

Chemical class: Phenylheptylamine
Therapeutic class: Synthetic opiate agonist

Pregnancy category: C

Controlled substance schedule: II

Indications

To manage opioid detoxification DISPERSIBLE , ORAL CONCENTRATE, I.M. OR SUBCUTANEOUS INJECTION
Adults.Initial: 15 to 40 mg daily or as needed. Usual: Dosage individualized based on clinical response. Maximum: 120 mg daily. Children.Dosage individualized based on age and size. Maximum: 120 mg daily. To maintain opioid abstinence DISPERSIBLE , ORAL CONCENTRATE
Adults.Dosage individualized based on clinical response. Maximum: 120 mg daily. Children. Dosage individualized based on age and size. Maximum: 120 mg daily. To treat severe or chronic pain ORAL CONCENTRATE,
Adults.5 to 20 mg every 4 to 8 hr. Dosage increased or dosing interval decreased, as prescribed and as needed. Maximum: 120 mg/day. Children. Dosage individualized based on age and size. , I.M.OR SUBCUTANEOUS INJECTION
Adults. 2.5 to 10 mg every 3 to 4 hr as needed. For chronic pain, dosage and dosing interval may be adjusted, as prescribed and as needed. Children.Dosage individualized based on age and size.
DOSAGE ADJUSTMENT Elderly patients, debilitated patients, and patients with severe hepatic or renal dysfunction, hypothyroidism, Addison’s disease, prostatic hyperplasia, or urethral stricture need individualized reduced dosages. Route Onset Peak Duration P.O. 30–60 min 1.5–2 hr 4–6 hr I.M. 10–20 min 1–2 hr 4–5 hr

Mechanism of Action

Binds with and activates opioid receptors (primarily mu receptors) in spinal cord and higher levels of CNS to produce analgesia and euphoric effects.

Contraindications

Acute or postoperative pain, acute or severe asthma, chronic respiratory disease, diarmethadone hydrochloride 640 rhea related to pseudomembranous colitis or poisoning, hypersensitivity to methadone or its components, respiratory depression, severe inflammatory bowel disease

Interactions

ammonium chloride, ascorbic acid, potassium, sodium phosphate: May precipitate methadone withdrawal symptoms amitriptyline, chloripramine, nortriptyline: Increased CNS and respiratory depression anticholinergics: Possibly severe constipation leading to ileus; urine retention antiemetics, general anesthetics, hypnotics, phenothiazines, sedatives, tranquilizers: Possibly coma, hypotension, respiratory depression, and severe sedation antihistamines, choral hydrate, glutethimide, MAO inhibitors, methocarbamol: Increased CNS and respiratory depressant effects of methadone antihypertensives, hypotension-producing : Increased hypotension, risk of orthostatic hypotension azole antifungals, macrolide antibiotics: Increased or prolonged opioid effect buprenorphine: Decreased therapeutic effect of methadone, increased respiratory depression, possibly withdrawal symptoms calcium channel blockers, class IA and class III antiarrhythmics, diuretics, laxatives, mineralocorticoid hormones, neuroleptics, tricyclic antidepressants: Increased risk of electrolyte disturbances and prolonged QT interval carbamazepine, phenobarbital, St. John’s wort: Possibly precipitation of withdrawal symptoms
cimetidine: Increased analgesic and CNS and respiratory depressant effects of methadone desipramine: Increased plasma desipramine level didanosine, stavudine: Decreased plasma levels of these diuretics: Decreased diuresis efavirenz, nevirapine, ritonavir, ritonavir and lopinavir: Decreased blood methadone level hydroxyzine: Increased analgesic, CNS depressant, and hypotensive effects of methadone loperamide, paregoric: Increased CNS depression, possibly severe constipation
MAO inhibitors: Possibly increased risk of severe

Side Efect

metoclopramide: Possibly antagonized metoclopramide effects on GI motility mixed agonist-antagonist analgesics: Possibly withdrawal symptoms naloxone: Antagonized analgesic and CNS and respiratory depressant effects of methadone, and possibly withdrawal symptoms
naltrexone: Possibly induction or worsening of withdrawal symptoms if methadone given within 7 days before naltrexone neuromuscular blockers: Increased or prolonged respiratory depression opioid analgesics (such as alfentanil and sufentanil): Increased CNS and respiratory depression, increased hypotension phenytoin,
rifampin: May precipitate withdrawal symptoms selective serotonin reuptake inhibitors: Possibly increased blood methadone levels and increased risk of methadone toxicity zidovudine: Increased blood zidovudine level and risk of toxicity
alcohol use: Increased CNS and respiratory depression, possibly hypotension

Side Efect

CNS: Agitation, amnesia, anxiety, asthenia, coma, confusion, decreased concentration, delirium, delusions, depression, dizziness, drowsiness, euphoria, fever, hallucinations, headache, insomnia, lethargy, light-headedness, malaise, psychosis, restlessness, sedation, seizures, syncope, tremor
CV: Bradycardia, cardiac arrest, cardiomyopathy, edema, heart failure, hypotension, orthostatic hypotension, palpitations, phlebitis, prolonged QT interval, shock, tachycardia, torsades de pointes, T-wave inversion on ECG, ventricular fibrillation or tachycardia
EENT: Blurred vision, diplopia, dry mouth, glossitis, laryngeal edema or laryngospasm (allergic), miosis, nystagmus, rhinitis
GI: Abdominal cramps or pain, anorexia, biliary tract spasm, constipation, diarrhea, dysphagia, elevated liver function test results, gastroesophageal reflux, hiccups, ileus and toxic megacolon (in patients with inflammatory bowel disease), indigestion, nausea, vomiting
GU: Amenorrhea, decreased ejaculate potency, decreased libido, difficult ejaculation, impotence, prolonged labor, urinary hesitancy, urine retention
HEME: Anemia, leukopenia, thrombocytopenia
MS: Arthralgia
RESP: Apnea, asthma exacerbation, atelectasis, bronchospasm, depressed cough reflex, hypoventilation, pulmonary edema, respiratory arrest and depression, wheezing
SKIN: Diaphoresis, flushing
Other: Allergic reaction; facial edema; hypokalemia; hypomagnesemia; injection site edema, pain, rash, or redness; physical and psychological dependence; weight gain; withdrawal symptoms

Cautions

Before giving methadone, make sure opioid antagonist and equipment for administering oxygen and controlling respiration are nearby.

Before therapy begins, assess patient’s current drug use, including all prescription and OTC .
WARNING Give drug cautiously to patients at risk for a prolonged QT interval, such as those with cardiac hypertrophy, hypokalemia, or hypomagnesemia; those with a history of cardiac conduction abnormalities; and those taking diuretics or medications that affect cardiac conduction.

Dilute oral concentrate with water or another liquid to volume of at least 30 ml, but preferably to 90 ml or more, before administration. Dissolve dispersible tablets in water or another liquid before giving.

Monitor patient for expected excessive drowsiness, unsteadiness, or confusion during first 3 to 5 days of therapy, and notify prescriber if effects continue to worsen or persist beyond this time.
WARNING Monitor respiratory and circulatory status carefully and often during methadone therapy because respiratory depression, circulatory depression, respiratory arrest, shock, hypotension, and cardiac arrest are risks. Monitor children often for respiratory depression and paradoxical CNS excitation because of their increased sensitivity to drug. Assess patient for excessive or persistent sedation; dosage may need to be adjusted.

Watch for drug tolerance, especially in patients with a history of chronic drug abuse, because methadone can cause physical and psychological dependence.

Monitor patient for pain because maintenance dosage doesn’t provide pain relief; patients with tolerance to opiate agonists, including those with chronic cancer pain, may require a higher dosage.

Monitor patients who are pregnant or who have liver or renal impairment for increased adverse effects from methadone because drug may have a prolonged duration and cumulative effect in these patients. Methadone may prolong labor by reducing strength, duration, and frequency of uterine contractions, so expect dosage to be tapered before third trimester of pregnancy. Breast-feeding mothers on maintenance therapy put their infants at risk of withdrawal symptoms if they abruptly stop breast-feeding or discontinue methadone therapy. Methadone also accumulates in CNS tissue, increasing the risk of seizures in infants.

Check plasma amylase and lipase levels in patients who develop biliary tract spasms because levels may increase up to 15 times normal. Notify prescriber immediately of any significant or sustained increase.

Monitor patients who have head injuries or other conditions that may increase intracranial pressure (ICP) because methadone may further increase ICP.

Assess patient for withdrawal symptoms and tolerance to therapy because physiologic dependence can occur with longterm methadone use. Avoid abrupt discontinuation because withdrawal symptoms will occur within 3 to 4 days after last dose.

Monitor patients, especially the elderly, for cardiac arrhythmias, hypotension, hypovolemia, orthostatic hypotension, and vasovagal syncope because methadone may produce cholinergic effects in patients with cardiac disease, resulting in bradycardia and peripheral vasodilation; dosage decrease may be indicated.

Monitor patients with prostatic hypertrophy, urethral stricture, or renal disease for urine retention and oliguria because methadone can increase tension of detrusor muscle.

Be prepared to treat patient’s symptoms of anxiety, and be aware that anxiety may be confused with symptoms of opioid abstimethadone hydrochloride 642 nence and that methadone doesn’t have antianxiety effects.

PATIENT SAFTY

Instruct patient taking oral concentrate form of methadone to dilute it with water or another liquid to a volume of at least 30 ml and preferably to 90 ml or more before administration.

Instruct patient to dissolve dispersible tablets in water or other liquid before administration.

Advise patient to notify prescriber of all other he’s currently taking and to avoid alcohol and other depressants, such as sleeping pills and tranquilizers, because they may increase drug’s CNS depressant effects.

Instruct patient to take drug only as prescribed and not to change dosage without prescriber approval. Inform patient that abrupt cessation of methadone therapy can precipitate withdrawal symptoms. Urge him to notify prescriber if he develops any concerns over therapy.

Urge patient to notify prescriber if he experiences palpitations, dizziness, lightheadedness, or syncope, which may be caused by methadone-induced arrhythmias.

Instruct patient to avoid potentially hazardous activities or those that require mental alertness because methadone therapy may cause drowsiness or sleepiness.

Teach patient to change positions slowly to minimize the effects of orthostatic hypotension.

Instruct patient to notify prescriber of worsening or breakthrough pain because dosage may need to be adjusted.

Inform parents that a child on methadone maintenance therapy may become unusually excited or restless; advise them to notify prescriber of changes in child’s behavior.

Instruct female patient to notify prescriber immediately if she becomes pregnant during methadone therapy because drug may cause physical dependence in fetus and withdrawal symptoms in neonate.

Caution patient who is breast-feeding not to stop doing so abruptly and not to stop taking methadone without prescriber’s approval because infant may experience withdrawal symptoms.

Category

Chemical class: Amphetamine
Therapeutic class: CNS stimulant

Pregnancy category: C

Controlled substance schedule: II

Indications

To treat attention-deficit hyperactivity disorder (ADHD) Children age 6 and over. 20 to 25 mg daily. Children age 6 and over. Initial: 5 mg once or twice daily. Increased by 5 mg every wk. Maintenance: 20 to 25 mg daily in divided doses b.i.d. Route Onset Peak Duration P.O. Unknown Unknown 6–24 hr

Mechanism of Action

May produce CNS stimulation by facilitating release and blocking reuptake of norepinephrine at adrenergic nerve terminals and by stimulating alpha and beta receptors in the peripheral nervous system. Methamphetamine also promotes dopamine release and blocks its reuptake in the brain’s limbic regions. It appears to act mainly in cerebral cortex and, possibly, reticular activating system. Its actions decrease motor restlessness, increase alertness, and reduce drowsiness and fatigue. Peripheral actions include increased blood pressure and mild bronchodilation and respiratory stimulation.

Contraindications

Advanced arteriosclerosis; glaucoma; hypersensitivity to methamphetamine, sympathomimetic amines, or their components; hyperthyroidism; history of drug abuse; moderate to severe hypertension; severe agitation; symptomatic cardiovascular disease; use within 14 days of MAO inhibitor

Interactions

ascorbic acid: Decreased methamphetamine absorption and therapeutic effect
beta blockers: Increased risk of heart block, hypotension, and severe bradycardia CNS stimulants: Increased CNS stimulation and risk of

Side Efect

digoxin, levodopa: Increased risk of arrhythmias diuretics, other antihypertensives: Possibly decreased antihypertensive effect ethosuximide, phenobarbital,
phenytoin: Possibly delayed absorption of these haloperidol, phenothiazines: Possibly interference with effects of these and with methamphetamine’s CNS stimulant effects inhalation anesthetics: Increased risk of ventricular arrhythmias insulin: Altered insulin requirements lithium: Possibly antagonized CNS stimulant effects of methamphetamine
MAO inhibitors: Possibly severe hypertension, risk of hypertensive crisis, increased vasopressor effect of methamphetamine meperidine: Increased risk of hypotension and life-threatening interactions, such as severe respiratory depression and coma metrizamide (intrathecal): Increased risk of seizures thyroid hormones: Enhanced effects of both tricyclic antidepressants: Increased risk of arrhythmias and severe hypertension urinary acidifiers: Increased metabolism and shortened pharmacologic effects of methamphetamine urinary alkalinizers: Decreased metabolism and prolonged pharmacologic effects of methamphetamine caffeine: Increased methamphetamine effects

Side Efect

CNS: Dizziness, euphoria, headache, hyperactivity, insomnia, irritability, mania, nervousness, psychotic episodes, restlessness, stroke, talkativeness, tremor
CV: Arrhythmias, chest pain, hypertension, hypotension, MI, palpitations, tachycardia
EENT: Accommodation abnormality, blurred vision, dry mouth, taste perversion
ENDO: Stunted growth
GI: Abdominal cramps, anorexia, constipation, diarrhea, nausea, vomiting
GU: Impotence, libido changes
SKIN: Diaphoresis, urticaria
Other: Physical and psychological dependence

Cautions

Methamphetamine shouldn’t be used in a patient (especially a child or an adolesccent) with a serious heart condition, such as a structural heart defect, cardiomyopathy, or a serious heart rhythm abnormality.

Use methamphetamine cautiously in patients with a history of psychiatric problems or suicidal or homicidal tendencies.

Assess for seizures in patients with a history of seizure disorders because drug may lower seizure threshold.

Observe patient for evidence of drug tolerance and, possibly, extreme dependence, which may develop after a few weeks. Be aware that methamphetamine abuse may occur.

Expect treatment for ADHD to include psychological, educational, and social measures in addition to drug therapy.

Monitor child’s growth pattern. If growth appears to be delayed, notify prescriber because methamphetamine therapy may need to be interrupted temporarily.

Watch for signs of chronic methamphetamine intoxication, including hyperactivity, insomnia, irritability, and personality changes. Notify prescriber if they occur.

Monitor patient for exertional chest pain, unexplained syncope, and other evidence that could suggest heart disease. If present, notify prescriber. A cardiac evaluation will be needed, and therapy may need to stop.

PATIENT SAFTY

Instruct parent of patient to give methamphetamine at least 6 hours before bedtime to prevent insomnia.

Explain high risk of abuse with this drug. Instruct parent of patient not to increase dosage unless advised by prescriber and not to give drug to prevent fatigue.
WARNING Advise patient to take methamphetamine exactly as prescribed because misuse may cause serious heart effects or even death.

Caution parent that patient should not crush or chew tablets.

Advise parent that patient should avoid caffeine, which increases drug’s effects.

Instruct parent of patient to report signs of overstimulation, such as diarrhea, hyperactivity, insomnia, and irritability.

Category

Chemical class: Sulfonamide derivative
Therapeutic class: Antiglaucoma

Pregnancy category: C

Indications

To treat open-angle glaucoma
Adults.50 to 100 mg b.i.d. or t.i.d. Route Onset Peak Duration P.O. 2–4 hr 6–8 hr 10–18 hr

Mechanism of Action

Inhibits the enyzme carbonic anhydrase, which normally appears in renal proximal tubule cells, choroid plexus of the brain, and ciliary processes of the eye. By inhibiting this enzyme in the eyes, methazolamide decreases aqueous humor secretion, which reduces intraocular pressure.

Contraindications

Cirrhosis; hyperchloremic acidosis; hypersensitivity to methazolamide, other carbonic anhydrase inhibitors, or their components; hypokalemia; hyponatremia; severe adrenocortical, hepatic, or renal impairment

Interactions

amphetamines, anticholinergics, mecamylamine, procainamide,
quinidine: Decreased renal clearance of these , increased risk of toxicity amphotericin B, corticosteroids: Increased risk of severe hypokalemia barbiturates, carbamazepine, phenytoin, primidone: Increased risk of osteopenia digoxin: Increased risk of hypokalemia and digitalis toxicity ephedrine: Possibly prolonged duration of action of ephedrine insulin, oral antidiabetic : Increased risk of glycosuria and hyperglycemia lithium: Increased lithium excretion mannitol: Increased diuresis and further reduction of intraocular pressure methenamine compounds: Decreased methenamine effectiveness
mexiletine: Possibly impaired renal excretion of mexiletine neuromuscular blockers: Possibly prolonged duration of action of blockers from methazolamide-induced hypokalemia, increased risk of prolonged respiratory paralysis and depression salicylates: Possibly CNS depression and metabolic acidosis, increased risk of methazolamide toxicity

Side Efect

CNS: Confusion, depression, drowsiness, fatigue, fever, malaise, paresthesia, seizures, weakness
EENT: Hearing loss, myopia (transient), taste perversion, tinnitus
GI: Anorexia, diarrhea, nausea, vomiting
GU: Crystalluria, nephrotoxicity, renal calculi
SKIN: Photosensitivity, pruritus, rash, Stevens-Johnson syndrome, urticaria
Other: Metabolic acidosis

Cautions

Use methazolamide cautiously in patients with obstructive pulmonary disease.

Monitor fluid intake and output, weight, and serum electrolyte levels during methazolamide therapy.

PATIENT SAFTY

Direct patient to take methazolamide exactly as prescribed because increasing dosage may lead to metabolic acidosis.

Advise patient to take drug with food if GI distress occurs.

Instruct patient to report if rash develops.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Emphasize need to have regular eye examinations during methazolamide therapy.

Category

Chemical class: Formaldehyde precursor, methazolamide; hexamethylenetetramine
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To prevent or suppress frequently recurring UTI caused by a wide variety of gram-negative and gram-positive bacteria (including enterococci, Escherichia coli, Micrococcus pyogenes, and staphylococci) in intermittently catheterized patients with neurogenic bladder ENTERIC-COATED , ORAL SUSPENSION (METHENAMINE MANDELATE) Adults and adolescents. 1 g q.i.d. before meals and at bedtime. Children ages 6 to 12. 500 mg q.i.d., or 50 mg/kg daily in divided doses. Children under age 6. 18.4 mg/kg q.i.d. (METHENAMINE HIPPURATE) Adults and adolescents.1 g b.i.d. Children ages 6 to 12. 0.5 to 1 g every 12 hr.

Mechanism of Action

Hydrolyzes to formaldehyde and ammonia in an acidic environment, such as urine, producing greater amounts of formaldehyde as pH decreases. Formaldehyde has bactericidal action, possibly by denaturing proteins. To facilitate hydrolysis, methenamine is formulated with weak organic acid, such as hippuric acid or mandelic acid.

Contraindications

Concurrent therapy with sulfonamides, hypersensitivity to methenamine, renal insufficiency, severe dehydration, severe hepatic disease

Interactions

bicarbonate-containing antacids, urinary alkalinizers: Decreased methenamine effect sulfonamides, such as sulfamethizole: Possibly formation of insoluble precipitate in urine milk, milk products, most fruits: Possibly decreased effectiveness of methenamine

Side Efect

CNS: Headache
CV: Edema
EENT: Stomatitis
GI: Abdominal cramps, anorexia, diarrhea, nausea, vomiting
GU: Bladder irritation, crystalluria, dysuria, hematuria, proteinuria, urinary frequency
RESP: Pulmonary hypersensitivity (dyspnea, pneumonitis)
SKIN: Pruritus, rash, urticaria

Cautions

Be aware that methenamine is used for prophylaxis; it isn’t recommended as primary treatment for UTI.

Drug shouldn’t be given to patients with creatinine clearance less than 50 ml/min/ 1.73 m2.

Before giving first dose, expect to obtain urine specimen for culture and sensitivity tests and to review test results if available.

Plan to give methenamine mandelate around the clock to maintain a therapeutic blood level.

Make sure patient receives adequate fluids.

Expect to repeat culture and sensitivity tests if patient fails to improve.

PATIENT SAFTY

Instruct patient to take methenamine with food to avoid GI distress.

Direct patient to drink extra fluids; avoid alkaline , such as milk, milk products, and most fruits; and avoid antacids that contain sodium bicarbonate or carbonate during methenamine therapy.

Instruct patient to report painful urination, rash, or severe GI distress.

Urge patient to comply with urine testing before and during long-term therapy.

Category

Chemical: Penicillinase-resistant penicillin
Therapeutic: Antibiotic

Pregnancy category: B

Indications

To treat general infections, such as sepsis, sinusitis, and skin and soft-tissue infections, caused by susceptible organisms (including penicillinase-producing and non–penicillinase-producing strains of Staphylococcus epidermidis, Staphylococcus saprophyticus, and Streptococcus pneumoniae)
IV:,
I.M.INJECTION Adults and children weighing 40 kg (88 lb) or more. 1 g every 4 to 6 hr (I.M.) or 1 g every 6 hr (I.V.). Maximum: 24 g daily. Children weighing less than 40 kg. 25 mg/ kg every 6 hr.
DOSAGE ADJUSTMENT For adults and children with cystic fibrosis, dosage adjusted to 50 mg/kg every 6 hr. To treat bacterial meningitis
IV:,
I.M.INJECTION Neonates weighing 2 kg (4.4 lb) or more. 50 mg/kg every 8 hr for first wk after birth and then 50 mg/kg every 6 hr. Neonates weighing less than 2 kg. 25 to 50 mg/kg every 12 hr for first wk after birth and then 50 mg/kg every 8 hr.

Mechanism of Action

Kills bacteria by inhibiting cell wall synthesis. In susceptible bacteria, the rigid, crosslinked cell wall is assembled in several steps. In final stage of cross-linking, methicillin binds with and inactivates penicillin-binding proteins (enzymes responsible for linking cell wall strands), resulting in bacterial cell lysis and death. Staphylococcus aureus has developed resistance to methicillin by altering its penicillin-binding proteins.

Incompatibilities

Don’t mix methicillin in same syringe or I.V. solution with other . Don’t mix methicillin with dextrose solutions because their low acidity may damage drug. Give methicillin at least 1 hour before or after aminoglycosides and at different sites; otherwise, mutual inactivation can occur.

Contraindications

Hypersensitivity to methicillin sodium, other penicillins, or their components

Interactions

aminoglycosides: Substantial aminoglycoside inactivation chloramphenicol, erythromycins, sulfonamides, tetracyclines: Possibly decreased therapeutic effects of methicillin methotrexate: Increased risk of methotrexate toxicity probenecid: Possibly decreased renal clearance, increased blood level, and increased risk of toxicity of methicillin

Side Efect

CNS: Aggressiveness, agitation, anxiety, confusion, depression, headache, seizures
EENT: Oral candidiasis
GI: Abdominal pain, diarrhea, hepatotoxicity, nausea, pseudomembranous colitis, vomiting
GU: Interstitial nephritis, vaginitis
HEME: Leukopenia, neutropenia, thrombocytopenia
SKIN: Exfoliative dermatitis, pruritus, rash, urticaria
Other: Anaphylaxis; infusion site redness, swelling, and tenderness; injection site pain, redness, and swelling; serum sicknesslike reaction

Cautions

WARNING Be aware that methicillin isn’t a first-line treatment for the indications above because of the prevalence of methicillin-resistant Staphylococcus aureus.

Before giving first dose, obtain appropriate body fluid or tissue specimens for culture and sensitivity tests, as ordered, and review test results if available.

Inject I.M. form deep into gluteal muscle.

In I.V. use, observe infusion site closely for redness, swelling, and tenderness.

Monitor fluid intake and output and renal function test results during therapy.

Observe for signs of superinfection, such as diarrhea, vaginal itching, and white patches or sores in mouth or on tongue. Notify prescriber if they occur.

Closely monitor renal function test results, including serum creatinine level; about one-third of patients have interstitial nephritis after 10 days of methicillin therapy.

Monitor liver function test results, and report evidence of hepatotoxicity, such as fever and nausea.

PATIENT SAFTY

Explain that I.M. injection may be painful.

Unless contraindicated, instruct patient to drink extra fluids during therapy.

Advise patient to report diarrhea, injection site pain, mouth sores, or rash.

Category

Chemical class: Thioimidazole derivative
Therapeutic class: Antithyroid

Pregnancy category: D

Indications

To treat mild hyperthyroidism Adults and adolescents.Initial: 15 mg daily as a single dose or in divided doses b.i.d. for 6 to 8 wk or until euthyroid level is reached. Maintenance: 5 to 30 mg daily as a single dose or in divided doses b.i.d. Children.Initial: 0.4 mg/kg daily as a single dose or in divided doses b.i.d. Maintenance: 0.2 mg/kg daily as a single dose or in divided doses b.i.d. To treat moderate hyperthyroidism Adults and adolescents. Initial: 30 to 40 mg/ day as a single dose or in divided doses b.i.d. for 6 to 8 wk or until euthyroid level is reached. Maintenance: 5 to 30 mg daily as a single dose or in divided doses b.i.d. Children.Initial: 0.4 mg/kg daily as a single dose or in divided doses b.i.d. Maintenance: 0.2 mg/kg daily as a single dose or in divided doses b.i.d. To treat severe hyperthyroidism Adults and adolescents. Initial: 60 mg daily as a single dose or in divided doses b.i.d. for 6 to 8 wk or until euthyroid level is reached. Maintenance: 5 to 30 mg daily as a single dose or in divided doses b.i.d. Children. Initial: 0.4 mg/kg daily as a single dose or in divided doses b.i.d. Maintenance: 0.2 mg/kg daily as a single dose or in divided doses b.i.d. As adjunct to treat thyrotoxicosis SUPPOSITORIES Adults and adolescents. 15 to 20 mg every 4 hr on first day and then adjusted based on patient response. Children. 0.4 mg/kg daily as a single dose or in divided doses b.i.d. Route Onset Peak Duration P.O. 5 days 7 wk Unknown

Mechanism of Action

Directly interferes with thyroid hormone synthesis in the thyroid gland by inhibiting iodide incorporation into thyroglobulin. Iodination of thyroglobulin is an important step in synthesizing the thyroid hormones thyroxine and triiodothyronine. Eventually, thyroglobulin is depleted and the circulating thyroid hormone level drops.

Contraindications

Breast-feeding; hypersensitivity to methimazole, other antithyroid , or their components

Interactions

amiodarone, iodine, potassium iodide: Decreased response to methimazole digoxin: Possibly increased blood digoxin level oral anticoagulants: Possibly a need for altered anticoagulant dosage

Side Efect

CNS: Drowsiness, headache, paresthesia, vertigo
CV: Edema
EENT: Loss of taste
ENDO: Hypothyroidism
GI: Diarrhea, indigestion, nausea, vomiting
HEME: Agranulocytosis, aplastic anemia, leukopenia, thrombocytopenia
MS: Arthralgia, myalgia
SKIN: Alopecia, jaundice, pruritus, rash, skin discoloration, urticaria
Other: Lupus-like symptoms, lymphadenopathy

Cautions

Closely monitor thyroid function test results during methimazole therapy.

Check CBC results to detect abnormalities caused by inhibition of myelopoiesis.

Watch for signs and symptoms of hypothyroidism, such as cold intolerance, depression, and edema.

Be aware that hyperthyroidism may increase metabolic clearance of beta blockers and theophylline and that dosages of these may need to be reduced as the patient’s thyroid condition becomes corrected.

PATIENT SAFTY

Instruct patient to take drug with meals to avoid adverse GI reactions.

Explain about possible hair loss or thinning during and for months after therapy.

Instruct patient to notify prescriber immediately about cold intolerance, fever, sore throat, tiredness, and unusual bleeding or bruising.

Category

Chemical class: Carbamate derivative of guaifenesin
Therapeutic class: Skeletal muscle relaxant

Pregnancy category: C

Indications

To relieve discomfort caused by acute, painful musculoskeletal conditions Adults and adolescents. Initial: 1,500 mg q.i.d. for 2 to 3 days; for severe discomfort, 8,000 mg daily. Maintenance: 750 mg every 4 hr, 1,000 mg q.i.d., or 1,500 mg t.i.d.
I.V.INJECTION(100 MG/ML) Adults and adolescents. Up to 3,000 mg daily administered at 8-hr intervals for 3 consecutive days. Regimen repeated as prescribed after patient is drug-free for 48 hr.

IM

(100 MG/ML) Adults and adolescents. 1,000 to 3,000 mg/ day administered at 8-hr intervals for 3 consecutive days. Regimen repeated as prescribed after patient is drug-free for 48 hr. To provide supportive therapy for tetanus Adults and adolescents.24,000 mg daily given by NG tube.
IV: OR INJECTION(100 MG/ML) Adults and adolescents.1,000 to 3,000 mg by infusion or 1,000 to 2,000 mg by direct injection every 6 hr. Maximum: 300 mg (3 ml)/min. Children.15 mg/kg every 6 hr. Route Onset Peak Duration P.O. 30 min Unknown Unknown I.V. Immediate Unknown Unknown

Mechanism of Action

May depress CNS, which leads to sedation and reduced skeletal muscle spasms. Methocarbamol also alters perception of pain.

Contraindications

Hypersensitivity to methocarbamol or its components, renal disease (injectable form)

Interactions

CNS depressants: Increased CNS depression
alcohol use: Increased CNS depression

Side Efect

CNS: Dizziness, drowsiness, fever, headache, light-headedness, seizures (I.V.), syncope, vertigo, weakness
CV: Bradycardia, hypotension, and thrombophlebitis (parenteral)
EENT: Blurred vision, conjunctivitis, diplopia, metallic taste, nasal congestion, nystagmus
GI: Nausea
GU: Black, brown, or green urine
SKIN: Flushing, pruritus, rash, urticaria
Other: Anaphylaxis (parenteral), angioedema, injection site irritation or pain (I.M.), injection site sloughing (I.V.)

Cautions

If needed, crush methocarbamol tablets and mix with water for administration by NG tube.

Give I.V. form directly through infusion line at 3 ml/min. To prepare solution, add 10 ml to no more than 250 ml D5W or normal saline solution. Infuse at no more than 300 mg (3 ml)/ min to avoid hypotension and seizures.

Keep patient recumbent during I.V. administration and for at least 15 minutes afterward. Then have him rise slowly.

Monitor I.V. site regularly for signs of phlebitis.

Inject I.M. form deep into large muscle, such as the gluteus. Give no more than 5 ml/dose every 8 hours. One dose is usually adequate.

Don’t give methocarbamol by subcutaneous route.

Keep epinephrine, antihistamines, and corticosteroids available in case patient experiences anaphylactic reaction.

Be aware that the parenteral dosage form shouldn’t be used in patients with renal dysfunction because the polyethylene glycol 300 vehicle is nephrotoxic.

PATIENT SAFTY

Tell patient to take drug exactly as prescribed.

Advise patient to take drug with food or milk to avoid nausea.

Inform patient that urine may turn green, black, or brown until mehtocarbamol is discontinued.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to avoid alcohol and other CNS depressants during therapy.

Category

Chemical class: Folic acid analogue
Therapeutic class: Antipsoriatic, antirheumatic

Pregnancy category: X

Indications

To treat severe psoriasis unresponsive to other therapy (METHOTREXATE)
Adults. 2.5 to 5 mg every 12 hr for 3 doses/ wk, increased as ordered by 2.5 mg/wk. Maximum: 20 mg/wk. I.V.OR
I.M.INJECTION(METHOTREXATE SODIUM)
Adults. 10 mg/wk. Maximum: 25 mg/wk. To treat severe rheumatoid arthritis unresponsive to other therapy (METHOTREXATE)
Adults. 2.5 to 5 mg every 12 hr for 3 doses/ wk, increased as ordered by 2.5 mg/wk. Maximum: 20 mg/wk. Route Onset Peak Duration P.O., I.V., 3–6 wk Unknown Unknown I.M.

Mechanism of Action

May exert immunosuppressive effects by inhibiting replication and function of T and possibly B lymphocytes. Methotrexate also slows rapidly growing cells, such as epithelial skin cells in psoriasis. This action may result from the drug’s inhibition of dihydrofolate reductase, the enzyme that reduces folic acid to tetrahydrofolic acid. Inhibition of tetrahydrofolic acid interferes with DNA synthesis and cell reproduction in rapidly proliferating cells.

Contraindications

Breast-feeding, hypersensitivity to methotrexate or its components, pregnancy

Interactions

bone marrow depressants: Possibly increased bone marrow depression co-trimoxazole: Possibly increased bone marrow suppression folic acid: Possibly decreased effectiveness of methotrexate hepatotoxic : Increased risk of hepatotoxicity chloramphenicol, neomycin, tetracycline: Possibly decreased methotrexate absorption NSAIDs, penicillins, phenylbutazone, phenytoin, probenecid, salicylates, sulfonamides: Increased risk of methotrexate toxicity oral anticoagulants: Increased bleeding risk sulfonamides: Increased risk of hepatotoxicity
theophylline: Possibly increased risk of theophylline toxicity vaccines: Risk of disseminated infection with live-virus vaccines, risk of suppressed response to killed-virus vaccines
alcohol use: Increased risk of hepatotoxicity

Side Efect

CNS: Aphasia, cerebral thrombosis, chills, dizziness, drowsiness, fatigue, fever, headache, hemiparesis, leukoencephalopathy, malaise, paresis, seizures
CV: Chest pain, deep vein thrombosis, hypotension, pericardial effusion, pericarditis, thromboembolism
ENDO: Gynecomastia
EENT: Blurred vision, conjunctivitis, gingivitis, glossitis, pharyngitis, stomatitis, transient blindness, tinnitus
GI: Abdominal pain, anorexia, cirrhosis, diarrhea, elevated liver function test results, enteritis, GI bleeding and ulceration, hepatitis, hepatotoxicity, nausea, pancreatitis, vomiting
GU: Cystitis, hematuria, infertility, menstrual dysfunction, nephropathy, renal failure, tubular necrosis, vaginal discharge
HEME: Anemia, aplastic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia
MS: Arthralgia, dysarthia, myalgia, stress fracture
RESP: Dry nonproductive cough, dyspnea, interstitial pneumonitis, pneumonia, pulmonary fibrosis or failure, pulmonary infiltrates
SKIN: Acne, alopecia, altered skin pigmentation, ecchymosis, erythema multiforme, exfoliative dermatitis, furunculosis, necrosis, photosensitivity, pruritus, psoriatic lesions, rash, Stevens-Johnson syndrome, telangiectasia, toxic epidermal necrolysis, ulceration, urticaria
Other: Anaphylaxis, increased risk of infection, lymphadenopathy, lymphoproliferative disease

Cautions

Follow facility policy for preparing and handling drug; parenteral form poses a risk of carcinogenicity, mutagenicity, and teratogenicity. Avoid skin contact.

Monitor results of CBC, chest X-ray, liver and renal function tests, and urinalysis before and during treatment.

Unless contraindicated, increase patient’s fluid intake to 2 to 3 L daily to reduce the risk of adverse GU reactions.

Assess patient for bleeding and infection.
WARNING Expect renal impairment to severely alter drug elimination.

Be aware that high doses of methotrexate can impair renal elimination by forming crystals that obstruct urine flow. To prevent drug precipitation, alkalinize patient’s urine with sodium bicarbonate tablets, as ordered.

Follow standard precautions because drug can cause immunosuppression.

If patient becomes dehydrated from vomiting, notify prescriber and expect to withhold drug until patient recovers.

If patient receives high doses of drug, keep leucovorin readily available as antidote.

Be aware that methotrexate resistance may develop with prolonged use.

PATIENT SAFTY

Prepare a calendar of treatment days for patient, and stress importance of following instructions exactly.

Instruct patient to avoid alcohol during methotrexate therapy.

Encourage frequent mouth care to reduce the risk of mouth sores.

Instruct patient to use sunblock when exposed to sunlight.

Advise patient to notify prescriber about bruising, chills, cough, fever, dark or bloody urine, mouth sores, shortness of breath, sore throat, and yellow skin or eyes.

Urge women of childbearing age to use reliable contraception during methotrexate therapy.

Category

Chemical class: Continuous erythropoietin receptor activator
Therapeutic class: Antianemic

Pregnancy category: C

Indications

To treat anemia associated with chronic renal failure in dialysis-dependent and dialysis-independent patients
I.V.INJECTION, SUBCUTANEOUS INJECTION Adults not currently being treated with an erythropoiesis-stimulating agent.Initial: 0.6 mcg/kg every 2 wk, increased or decreased by 25% monthly as needed. Maintenance: 1.2 mcg/kg every 4 wk. Adults stabilized on less than 8,000 units/ wk of epoetin alfa or 40 mcg/wk of darbepoetin alfa. 60 mcg every 2 wk or 120 mcg every 4 wk. Adults stabilized on 8,000 to 16,000 units/ wk of epoetin alfa or 40 to 80 mcg/wk of darbepoetin alfa. 100 mcg every 2 wk or 200 mcg every 4 wk. Adults stabilized on more than 16,000 units/wk of epoetin alfa or more than 80 mcg/wk of darbepoetin alfa. 180 mcg every 2 wk or 360 mcg every 4 wk.
DOSAGE ADJUSTMENT If hemoglobin increase is greater than 1 g/dl during any 2wk period or hemoglobin is increasing and approaching 12 g/dl, dosage reduced by 25%. If hemoglobin continues to increase despite this reduction, drug discontinued until hemoglobin begins to decrease; then drug restarted at a dose 25% less than previously given. If hemoglobin doesn’t methoxypolyethylene glucol-epoetin beta increase by 1 g/dl after 4 wk of therapy, dosage increased by 25%.

Mechanism of Action

Stimulates release of reticulocytes from bone marrow into the bloodstream, where they develop into mature RBCs.

Incompatabilities

Don’t mix methoxypolyethylene glycol-epoetin beta with any other drug.

Contraindications

Hemoglobin greater than 12 g/dl, hypersensitivity to methoxypolyethylene glycolepoetin beta or its components, red cell aplasia, uncontrolled hypertension

Side Efect

CNS: Headache, seizures, stroke
CV: Chest pain, congestive heart failure, deep vein thrombosis, hypertension, hypotension, MI, tachycardia, vascular access thrombosis
EENT: Nasopharyngitis
GI: Constipation, diarrhea, GI bleeding, vomiting
GU: UTI
HEME: Pure red cell aplasia, severe anemia
MS: Back or limb pain, muscle spasms
RESP: Cough, upper respiratory tract infection
SKIN: Erythema, pruritus, rash
Other: Anaphylaxis, antibody formation to drug

Cautions

Use drug cautiously in patients who have conditions that could decrease or delay response to drug, such as aluminum intoxication, folic acid deficiency, hemolysis, infection, inflammation, iron deficiency, malignant neoplasm, osteitis (birrosa cystica), or vitamin B12deficiency.

Also use drug cautiously in patients with a cardiovascular disorder caused by hypertension, a history of seizures, vascular disease, or a hematologic disorder, such as hypercoagulation, myelodysplastic syndrome or sickle cell disease.

Be aware that if patient’s blood pressure is difficult to control even with drug therapy or dietary measures, dose of methoxypolyethylene glycol-epoetin beta should be reduced or drug withheld until blood pressure is controlled.

Don’t shake vial during preparation to avoid denaturing glycoprotein, inactivating drug. Protect vials and prefilled syringes from light by storing in original cartons.

Discard unused portion of single-dose vial because it contains no preservatives.
WARNING Target hemoglobin shouldn’t exceed 12 g/dl because it increases risk of life-threatening adverse cardiovascular effects.

Monitor drug effectiveness by checking hemoglobin every 2 weeks until stabilized at 10 to 12 g/dl and maintenance dose has been established. Then expect hemoglobin to be monitored at least monthly unless
DOSAGE ADJUSTMENT is needed.

Expect to give an iron supplement because iron requirements rise when erythropoiesis consumes existing iron stores.

Notify prescriber if patient has sudden loss of response to drug, evidenced by severe anemia and a low reticulocyte count. Antierythropoietin antibody-related anemia may be present, which requires stopping drug and any other erythropoietic proteins.

Take seizure precautions, especially during the first couple months of therapy.

Risk of hypertensive or thrombotic complications increases if hemoglobin rises more than 1 g/dl over 2 weeks.

PATIENT SAFTY

Teach patient how to administer drug and how to dispose of needles properly. Caution against reusing needles.

Stress importance of complying with dosage regimen and keeping follow-up medical and laboratory appointments.

Review possible

Side Efect

, and urge patient to notify prescriber about chest pain, headache, hives, rapid heartbeat, rash, seizures, shortness of breath, or swelling.

Advise patient that the risk of seizures is highest during the first couple of months of methoxypolyethylene glycol-epoetin beta therapy. Urge him to avoid hazardous activities during this time.

Encourage patient to eat iron-rich

Category

Chemical class: Quaternary ammonium derivative of scopolamine
Therapeutic class: Anticholingeric

Pregnancy category: C

Indications

As adjunct to treat peptic ulcer
Adults.For mild to moderate symptoms, 2.5 mg 30 min before meals and 2.5 to 5 mg at bedtime; for severe symptoms, 5 mg 30 min. before meals and at bedtime.

Mechanism of Action

Reduces volume and total acid content of gastric secretions, which may have a beneficial effect in treating peptic ulcer. Drug also reduces GI motility and inhibits salivation, which may have additional benefits.

Contraindications

Glaucoma, hypersensitivity to methscopolamine bromide or its components, intestinal atony (elderly or debilitated patients), myasthenia gravis, obstructive disease of GI or GU tract, paralytic ileus, severe ulcerative colitis, toxic megacolon complicating ulcerative colitis, unstable cardiovascular status in acute hemorrhage

Interactions

antacids: Possibly decreased methscopolamine absorption anticholinergics, antipsychotics, tricyclic antidepressants: Possibly increased anticholinergic effects

Side Efect

CNS: Confusion, dizziness, drowsiness, headache, insomnia, nervousness, weakness
CV: Palpitations, tachycardia
EENT: Blurred vision, cycloplegia, dry mouth, increased intraocular pressure, loss of taste, pupil dilation
ENDO: Suppression of lactation
GI: Bloating, constipation, nausea, vomiting
GU: Impotence, urinary hesitancy, urine retention
SKIN: Decreased sweating, urticaria
Other: Anaphylaxis

Cautions

Use with caution in elderly patients and in patients with autonomic neuropathy, congestive heart failure, coronary artery disease, hepatic or renal disease, hypertension, hyperthyroidism, prostatic hypertrophy, tachycardia, or ulcerative colitis.

Notify prescriber if diarrhea occurs because it may be an early sign of incomplete intestinal obstruction.

PATIENT SAFTY

Advise patient to avoid excessive exposure to heat to reduce the risk of heat prostration and heatstroke because methscopolamine decreases sweating.

Caution patient to avoid antacids because they may interfere with drug’s absorption.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Category

Chemical class: Succinimide derivative
Therapeutic class: Anticonvulsant

Pregnancy category: Not rated

Indications

To treat absence seizures unresponsive to other Adults and children.Initial: 300 mg daily. Increased by 150 to 300 mg daily every 1 to 2 wk until control is achieved with minimal

Side Efect

. Maximum: 1.2 g daily in divided doses.

Mechanism of Action

Elevates seizure threshold and reduces frequency of seizures by depressing motor cortex and elevating threshold of CNS response to convulsive stimuli. Methsuximide is metabolized to active metabolite Ndemethylmethsuximide, which may add to the anticonvulsant effects of the drug.

Contraindications

Hypersensitivity to methsuximide, succinimides, or their components

Interactions

carbamazepine, phenobarbital, phenytoin, primidone: Possibly decreased blood methsuximide level
CNS depressants: Possibly increased CNS depression
haloperidol: Altered seizure pattern; possibly decreased blood haloperidol level loxapine, MAO inhibitors, maprotiline, molindone, phenothiazines, pimozide, thioxanthenes, tricyclic antidepressants: Possibly lowered seizure threshold and reduced therapeutic effect of methsuximide
alcohol use: Possibly increased CNS depression

Side Efect

CNS: Aggressiveness, ataxia, decreased concentration, dizziness, drowsiness, fatigue, fever, headache, insomnia, irritability, mental depression, nightmares, seizures, suicidal ideation
EENT: Periorbital edema, pharyngitis
GI: Abdominal and epigastric pain, abdominal cramps, abnormal liver function test results, anorexia, diarrhea, hiccups, nausea, vomiting
GU: Microscopic hematuria, proteinuria
HEME: Agranulocytosis, aplastic anemia, eosinophilia, leukopenia, pancytopenia
MS: Muscle pain
SKIN: Erythematous and pruritic rash, Stevens-Johnson syndrome, systemic lupus erythematosus, urticaria
Other: Lymphadenopathy

Cautions

Monitor CBC and platelet count and assess patient for signs of infection, such as cough, fever, and pharyngitis, because methsuximide may cause blood dyscrasias.

Monitor liver function test results and urinalysis results in patients with a history of hepatic or renal disease; methsuximide may cause functional changes in liver and kidneys.

When giving drug to patient with a history of mixed-type epilepsy, institute seizure precautions because drug may increase risk of generalized tonic-clonic seizures.

Expect the dosage to be carefully and slowly adjusted according to patient’s response and needs and withdrawn slowly to avoid precipitating seizures.

Plan to use 150-mg capsule when making
DOSAGE ADJUSTMENTs for small children.

Notify prescriber if patient develops depression or aggressiveness.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

PATIENT SAFTY

Advise patient to take a missed dose as soon as he remembers unless it’s nearly time for the next dose. Warn him not to double the dose.

Instruct patient to take drug with milk or food to reduce gastric irritation.

Advise patient to notify prescriber if he develops cough, fever, or pharyngitis.

Urge patient to avoid alcohol because of increased risk of CNS depression.

Instruct patient to avoid hazardous activities until drug’s adverse effects are known.

Caution patient not to stop taking drug abruptly to avoid risk of absence seizures.

Category

Chemical class: 3,4-dihydroxyphenylalanine (DOPA) analogue
Therapeutic class: Antihypertensive methyldopa 654

Pregnancy category: B

(oral form), C (parenteral form)

Indications

To manage hypertension, to treat hypertensive crisis ORAL SUSPENSION
Adults.Initial: 250 mg b.i.d. or t.i.d. for first 48 hr, increased as ordered after 2 days. Maintenance: 500 to 2,000 mg daily in divided doses b.i.d. to q.i.d. Maximum: 3,000 mg daily. Children.Initial: 10 mg/kg daily in divided doses b.i.d. to q.i.d. for first 48 hr, increased as ordered after 2 days. Maximum: 65 mg/ kg or 3,000 mg daily.
IV:
Adults.250 to 500 mg diluted in D5W and infused over 30 to 60 min every 6 hr. Maximum: 1,000 mg every 6 hr. Children. 20 to 40 mg/kg infused over 30 to 60 min every 6 hr. Maximum: 65 mg/ kg or 3,000 mg daily. Route Onset Peak Duration P.O. Unknown 4–6 hr* 12–24 hr I.V. Unknown 4–6 hr 10–16 hr

Mechanism of Action

Is decarboxylated in the body to produce alpha-methylnorepinephrine, a metabolite that stimulates central inhibitory alphaadrenergic receptors. This action may reduce blood pressure by decreasing sympathetic stimulation of heart and peripheral vascular system.

Incompatibilities

Don’t administer methyldopa through same I.V. line as barbiturates or sulfonamides.

Contraindications

Active hepatic disease, hypersensitivity to methyldopa or its components, impaired hepatic function from previous methyldopa therapy,use within 14 days of MAO inhibitor

Interactions

antihypertensives: Increased hypotension appetite suppressants, NSAIDs, tricyclic antidepressants: Possibly decreased therapeutic effects of methyldopa central anesthetics: Possibly need for reduced anesthetic dosage
CNS depressants: Possibly increased CNS depression
haloperidol: Increased risk of adverse CNS effects levodopa: Possibly decreased therapeutic effects of levodopa and increased risk of adverse CNS effects lithium: Increased risk of lithium toxicity
MAO inhibitors: Possibly hallucinations, headaches, hyperexcitability, and severe hypertension oral anticoagulants: Possibly increased therapeutic effects of anticoagulants sympathomimetics: Possibly decreased therapeutic effects of methyldopa and increased vasopressor effects of sympathomimetics
alcohol use: Possibly increased CNS depression

Side Efect

CNS: Decreased concentration, depression, dizziness, drowsiness, fever, headache, involuntary motor activity, memory loss (transient), nightmares, paresthesia, parkinsonism, sedation, vertigo, weakness
CV: Angina, bradycardia, edema, heart failure, myocarditis, orthostatic hypotension
EENT: Black or sore tongue, dry mouth, nasal congestion
ENDO: Gynecomastia
GI: Constipation, diarrhea, flatulence, hepatic necrosis, hepatitis, nausea, pancreatitis, vomiting
GU: Decreased libido, impotence
HEME: Agranulocytosis, hemolytic anemia, leukopenia, positive Coombs’ test, positive tests for ANA and rheumatoid factor, thrombocytopenia
SKIN: Eczema, rash, urticaria
Other: Weight gain

Cautions

For I.V. infusion, add methyldopate to 100 ml of D5W and administer over 30 to 60 minutes.

Expect to monitor CBC and differential results before and periodically during methyldopa therapy.

Monitor blood pressure regularly during therapy. * For single dose; 2 to 3 days for multiple doses. For single dose; 24 to 48 hr for multiple doses.

Monitor results of Coombs’ test; a positive result after several months of treatment indicates that patient has hemolytic anemia. Expect to discontinue drug.

Assess for weight gain and edema. If they develop, give a diuretic, as prescribed.

Notify prescriber if patient has signs of heart failure (dyspnea, edema, hypertension) or involuntary, rapid, jerky movements.

Be aware that hypertension may return within 48 hours after stopping drug.

PATIENT SAFTY

Instruct patient to take methyldopa exactly as prescribed and not to skip a dose. Explain that hypertension can return within 48 hours after stopping drug.

Suggest that patient take drug at bedtime to minimize daytime drowsiness.

Instruct patient to weigh himself daily and to report a gain of more than 5 lb (2.3 kg) in 2 days.

Advise patient to change position slowly to minimize orthostatic hypotension.

Direct patient to notify prescriber about bruising, chest pain, fever, involuntary jerky movements, prolonged dizziness, rash, and yellow eyes or skin.

Caution patient not to stop drug abruptly; doing so may cause withdrawal symptoms, such as headache, hypertension, increased sweating, nausea, and tremor.

Category

Chemical class: Noroxymorphone methobromide
Therapeutic class: Peripheral mu-opioid receptor antagonist

Pregnancy category: B

Indications

To treat opioid-induced constipation in patients receiving palliative care and not responsive to laxative therapy. SUBCUTANEOUS INJECTION Adults weighing more than 114 kg (251 lb): 0.15 mg/kg every other day as needed. Maximum: 0.15 mg/kg daily. Adults weighing 62 to 114 kg (136 to 251 lb): 12 mg every other day as needed. Maximum: 12 mg daily. Adults weighing 38 to less than 62 kg (84 to less than 136 lb): 8 mg every other day as needed. Maximum: 8 mg daily. Adults weighing less than 38 kg: 0.15 mg/ kg every other day as needed. Maximum: 0.15 mg/kg daily.
DOSAGE ADJUSTMENT For patients with severe renal failure (creatinine clearance less than 30 ml/min/1.73 m2), dosage reduced by half. Route Onset Peak Duration SubQ Unknown 0.5 hr Unknown

Mechanism of Action

Binds to peripherally acting mu-opioid receptors in the GI tract, preventing opioidinduced slowing of GI transit time and motility. When transit time and motility is restored to normal, constipation is relieved.

Contraindications

Hypersensitivity to methylnaltrexone bromide or its components, I.V. administration, mechanical GI obstruction

Side Efect

CNS: Dizziness
GI: Abdominal pain, diarrhea, flatulence, nausea Skin: Diaphoresis

Cautions

To determine volume of drug to give patients who weigh more than 114 kg (251 lb) or less than 38 kg (84 lb), multiply patient’s weight in pounds by 0.0034 and round up to the nearest 0.1 ml. Or. multiply patient’s weight in kilograms by 0.0075 and round up to the nearest 0.1 ml. For patients who weigh 62 to 114 kg (136 to 251 lb), injection volume administered should be 0.6 ml. For patients who weigh 38 to less than 62 kg (84 to less than 136 lb), injection volume administered should be 0.4 ml.

Inspect vial before giving drug to make sure solution is clear and colorless to pale yellow.

Give drug only as subcutaneous injection into patient’s upper arm, abdomen, or thigh and no more than once in 24 hours. Make sure to rotate injection sites.

Once drug is drawn into syringe, it should be given immediately. However, if needed, it may be stored at room temperature for up to 24 hours.

Notify prescriber about severe or persistent diarrhea, and expect drug to be discontinued.

PATIENT SAFTY

Teach patient or caregiver how to prepare and give methylnaltrexone subcutaneously. Stress need to rotate injection sites.

Inform patient that a bowel movement may occur within 30 minutes after drug has been administered.

Advise patient that if severe or persistent diarrhea occurs, prescriber should be notified and drug discontinued.

Reassure patient that drug is not a controlled substance.

Tell patient to stop taking methylnaltrexone if she stops taking opioid pain medication.

Category

Chemical class: Piperidine derivative
Therapeutic class: CNS stimulant

Pregnancy category: C

Controlled substance schedule: II

Indications

To treat attention-deficit hyperactivity disorder (ADHD) , ,, S.R., Adults and adolescents. 5 to 20 mg b.i.d. or t.i.d. Maximum: 90 mg daily. Children ages 6 to 12. 5 mg b.i.d. before breakfast and lunch; increased by 5 to 10 mg daily at 1-wk intervals. Maximum: 60 mg daily. ONCE-DAILY (CONCERTA) Adults and adolescents. 18 mg daily; increased in 18-mg increments at 1-wk intervals. Maximum: 72 mg daily, not to exceed 2 mg/kg daily. Children ages 6 to 12. 18 mg daily. Maximum: 54 mg daily. ONCE-DAILY (METADATE CD) Children age 6 and over. 20 mg daily. Dosage titrated to 40 or 60 mg daily based on individual response. Maximum: 60 mg daily.
DOSAGE ADJUSTMENT Dosage reduced or drug stopped if no improvement in 1 mo. When maintenance dosage is achieved with tablets, may be switched to or S.R. tablets. TRANSDERMAL PATCH Children ages 6 to 12. Initial: 10-mg (12.5cm2) patch worn 9 hr daily; after 1 wk, increased to 15-mg (18.75-cm2) patch worn 9 hr daily; after 1 more wk, increased to 20-mg (25-cm2) patch worn 9 hr daily; after 1 more wk, increased to 30-mg (37.5cm2) patch worn 9 hr daily. Maximum: 30mg (37.5-cm2) patch worn 9 hr daily. To treat narcolepsy

ORALL

, Adults and adolescents. 5 to 20 mg b.i.d. or t.i.d. Maximum: 90 mg daily. Route Onset Peak Duration P.O. Unknown Unknown 3–6 hr (tablets) P.O. Unknown Unknown About (, S.R.) 8 hr P.O. Unknown Unknown About ( 12 hr once-daily)

Mechanism of Action

Blocks the reuptake mechanism of dopaminergic neurons in the cerebral cortex and subcortical structures of the brain, including the thalamus, decreasing motor restlessness and improving concentration. Methylphenidate also may trigger sympathomimetic activity. This action produces increased motor activity, alertness, mild euphoria, and decreased fatigue in patients with narcolepsy.

Contraindications

Angina pectoris, anxiety, cardiac arrhythmias, depression, fructose intolerance, glaumethylphenidate hydrochloride 657 M coma, glucose-galactose malabsorption, heart failure, hypersensitivity to methylphenidate or its components, hyperthyroidism, motor tics, recent MI, severe agitation, severe hypertension, sucrase-isomaltase insufficiency, tension, thyrotoxicosis, Tourette’s syndrome or family history of it, use of halogenated anethestics, use within 14 days of an MAO inhibitor

Interactions

anticholinergics: Possibly increased anticholinergic effects of both anticonvulsants, oral anticoagulants, phenylbutazone, tricyclic antidepressants: Inhibited metabolism and increased blood levels of these diuretics, antihypertensives: Decreased therapeutic effects of these halogenated anesthetics: Possibly sudden decrease in blood pressure during surgery
MAO inhibitors: Possibly increased adverse effects of methylphenidate, possibly severe hypertension caffeine: Increased methylphenidate effects

Side Efect

CNS: Agitation, aggressiveness, anxiety, confusion, depression, dizziness, dyskinesia, emotional lability, fever, hallucinations, headache, hyperactivity, insomnia, irritability, ischemic neurologic defects (reversible), mania, migraine, motor tics, nervousness, obsessive-compulsive disorder, paresthesia, psychosis, sedation, seizures, stroke, suicidal ideation, transient mood depression, tension, tremor, Tourette’s syndrome, vertigo
CV: Angina, arrhythmias, bradycardia, cardiac arrest, chest pain, extrasystoles, hypertension, hypotension, MI, palpitations, Raynaud’s phenomenon, sudden death, tachycardia
EENT: Accommodation abnormality, blurred vision, diplopia, dry mouth or throat, mydriasis, pharyngitis, rhinitis, sinusitis, vision changes
ENDO: Dysmenorrhea, growth suppression in children with long-term use
GI: Abdominal pain, anorexia, constipation, diarrhea, dyspepsia, hepatotoxicity, nausea, vomiting
GU: Decreased libido
HEME: Anemia, decreased platelet count, leukopenia, pancytopenia, thrombocytopenia, thrombocytopenic purpura
MS: Arthralgia, myalgia, muscle tightness or twitching
RESP: Increased cough, upper respiratory tract infection
SKIN: Allergic contact dermatitis, alopecia, application site reactions (transdermal patch), diaphoresis, erythema multiforme, exfoliative dermatitis, pruritus, rash, urticaria
Other: Anaphylaxis, angioedema, physical and psychological dependence, weight loss

Cautions

WARNING Be aware that methylphenidate may induce CNS stimulation and psychosis and may worsen behavior disturbances and thought disorders in patients who already have psychosis. Use drug cautiously in patients with psychosis.

Keep in mind that, when signs and symptoms of ADHD occur with acute stress reactions or with pre-existing structural cardiac abnormalities or other serious heart problems, methylphenidate usually isn’t indicated because of possible worsened reaction or sudden death.

Monitor children and adolescents for firsttime psychotic or manic symptoms. If present, notify prescriber and expect drug to be discontinued.
WARNING Know that the tablet form (Concerta) shouldn’t be given to patients with esophageal motility disorders; drug may cause GI obstruction because tablet doesn’t change shape in GI tract.

Monitor blood pressure and pulse rate to detect hypertension and excessive stimulation. Notify prescriber if present. For patient with hypertension, expect to increase antihypertensive dosage or add another antihypertensive to regimen.
WARNING Watch for signs of physical or psychological dependence. Methylphenidate’s abuse potential is similar to that of amphetamines; use cautiously in patients with a history of drug abuse.

Stopping drug abruptly after long-term use may unmask dysphoria, paranoia, severe depression, or suicidal thoughts.

Monitor growth in children. Report failure to grow or gain weight, and expect to stop drug.

Watch closely (especially children, adolescents, and young adults), for suicidal tendencies, particularly when therapy starts and dosage changes, because depression may worsen temporarily during these times, possibly leading to suicidal ideation.

Monitor transdermal patch application site for erythema. If more intense reactions occur with erythema, such as local edema or papule or vesicle formation that don’t improve within 48 hours after patch is removed from irritated site or that spread beyond the patch site, expect further diagnostic testing to determine presence of allergic contact dermatitis.

Patients with allergic contact dermatitis from transdermal patch may develop systemic allergy reaction if methylphenidate is taken by another route, such as by mouth. Monitor patient closely if route of administration changes, and report any evidence of flare-up of previous dermatitis or positive patch-test sites, generalized skin eruptions in previously unaffected skin, headache, fever, malaise, arthralgia, diarrhea, or vomiting because drug may need to be discontinued.

PATIENT SAFTY

Stress need to take drug exactly as prescribed because misuse may cause serious adverse cardiovascular reactions, including sudden death.

For transdermal form, teach patient to apply patch to a clean, dry location in his hip area 2 hours before effect is needed and to remove it 9 hours after application.

Caution patient to avoid applying patch to skin that’s oily, damaged, or irritated and to avoid the waistline, where clothing may dislodge the patch. Tell patient to rotate application sites between hips.

Instruct patient to apply patch immediately after opening pouch and removing protective liner. Tell him to press patch firmly in place with palm of his hand for about 30 seconds. Reassure patient that exposing site to water shouldn’t cause patch to fall off. If a patch does fall off, explain that a new patch may be applied but that the total exposure time for the day shouldn’t exceed 9 hours.

Urge patient not to chew or crush tablets.

Tell patient to take tablets at least 6 hours before bedtime to avoid insomnia and to take once-daily tablets in the morning.

Advise patient taking once-daily tablets (Concerta) that he may see intact tablet in stool. Explain that drug is slowly released from nonabsorbable tablet shell.

Tell patient taking capsule form to swallow it whole or sprinkle contents onto a tablespoon of applesauce and take immediately, followed by a liquid such as water.

Direct patient to notify prescriber about excessive nervousness, fever, insomnia, palpitations, rash, or vomiting.

Warn patient with seizure disorder that drug may cause seizures.

Inform parents of children on long-term therapy that drug may delay growth.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes and particularly if patient is a child, teenager, or young adult.

Category

Chemical class: Synthetic glucocorticoid
Therapeutic class: Anti-inflammatory, immunosuppressant

Pregnancy category: C

Indications

To treat ulcerative colitis
IV:
Adults.40 to 120 mg 3 to 7 times/wk for 2 or more wk. Later doses given I.V. or I.M., based on patient’s condition and response. Children.0.14 to 0.84 mg/kg daily in dividmethylprednisolone 659 M ed doses every 12 to 24 hr. To treat a wide range of immune and inflammatory disorders, including allergic rhinitis, asthma, Crohn’s disease, and systemic lupus erythematosus
Adults.4 to 48 mg daily as a single dose or in divided doses. Children.0.42 to 1.67 mg/kg daily in divided doses t.i.d. or q.i.d.
IV:,
I.M.INJECTION
Adults. Initial: 10 to 40 mg infused over several min. Later doses given I.V. or I.M., based on patient’s condition and response. Children.0.14 to 0.84 mg/kg every 12 to 24 hr.

IM

Adults. 40 to 120 mg daily to every 2 wk, according to clinical response. Children. 0.14 to 0.84 mg/kg every 12 to 24 hr. INTRA-ARTICULAR, INTRALESIONAL, OR SOFTTISSUE INJECTION
Adults. 4 to 80 mg every 1 to 5 wk, according to clinical response. To treat adrenal hyperplasia

IM

(
Adults. 40 mg every 2 wk. Children. 0.14 to 0.84 mg/kg every 12 to 24 hr. To treat acute exacerbations of multiple sclerosis
Adults.160 mg daily for 7 days followed by 64 mg every other day for 1 mo. I.V.OR
I.M.INJECTION
Adults.160 mg daily for 1 wk followed by 64 mg every other day for 1 mo. To treat adrenocortical insufficiency ,
I.M.INJECTION Children.0.18 mg/kg daily in divided doses t.i.d.

IM

Children.0.12 mg/kg every 3 days or 0.039 to 0.059 mg/kg daily.

Mechanism of Action

Binds to intracellular glucocorticoid receptors and suppresses inflammatory and immune responses by inhibiting accumulation of neutrophils and monocytes at inflammation sites, stabilizing lysosomal membranes, suppressing the antigen response of macrophages and helper T cells, and inhibiting the synthesis of inflammatory response mediators, such as cytokines, interleukins, and prostaglandins. Route Onset Peak Duration P.O. In 60 min 1–2 hr 1.25–1.5 days I.V. Rapid 30 min Unknown I.M. 6–48 hr 4–8 days 1–4 wk

Incompatibilities

Don’t mix methylprednisolone with any drug without first consulting pharmacist. Don’t dilute methylprednisolone acetate with any other drug.

Contraindications

Fungal infection, hypersensitivity to methylprednisolone or its components, idiopathic thrombocytopenic purpura (I.M.)

Interactions

acetaminophen: Increased risk of hepatotoxicity aminoglutethimide: Possibly loss of methylprednisolone-induced adrenal suppression amphotericin B, carbonic anhydrase inhibitors: Possibly severe hypokalemia anabolic steroids, androgens: Increased risk of edema and worsening of acne anticholinergics: Possibly increased intraocular pressure asparaginase: Increased risk of hyperglycemia and toxicity aspirin,
NSAIDs: Increased risk of adverse GI effects and bleeding barbiturates, carbamazepine, phenytoin,
rifampin: Decreased blood methylprednisolone level cholestyramine: Possibly increased methylprednisolone clearance cyclosporine: Increased risk of seizures digoxin: Possibly hypokalemia-induced arrhythmias and digitalis toxicity estrogens, oral contraceptives: Possibly increased therapeutic and toxic effects of methylprednisolone insulin, oral antidiabetic : Possibly increased blood glucose level isoniazid: Possibly decreased therapeutic effects of isoniazid ketoconazole, macrolide antibiotics such as erythromycin and troleandomycin: Decreased methylprednisolone clearance and increased risk of adverse effects
mexiletine: Possibly decreased blood mexiletine level neuromuscular blockers: Possibly increased neuromuscular blockade, causing respiratory depression or apnea oral anticoagulants, thrombolytics: Increased risk of GI ulceration and hemorrhage, possibly decreased therapeutic effects of these potassium supplements: Possibly decreased effects of these supplements somatrem, somatropin: Possibly decreased therapeutic effects of these streptozocin: Increased risk of hyperglycemia troleandomycin: Increased blood methylprednisolone level vaccines: Decreased antibody response and increased risk of neurologic complications
alcohol use: Increased risk of adverse GI effects and bleeding

Side Efect

CNS: Ataxia, behavioral changes, depression, dizziness, euphoria, fatigue, headache, increased intracranial pressure with papilledema, insomnia, malaise, mood changes, neuropathy, paresthesia, restlessness, seizures, steroid psychosis, syncope, vertigo
CV: Arrhythmias (from hypokalemia), cardiac arrest, edema, fat embolism, heart failure, hypertension, hypertrophic cardiomyopathy (premature infants), hypotension, myocardial rupture following recent MI, tachycardia, thromboembolism, thrombophlebitis
EENT: Exophthalmos, glaucoma, increased intraocular pressure, nystagmus, posterior subcapsular cataracts
ENDO: Adrenal insufficiency, cushingoid symptoms (moon face, buffalo hump, central obesity, supraclavicular fat pad enlargement), diabetes mellitus, growth suppression in children, hyperglycemia, negative nitrogen balance from protein catabolism
GI: Abdominal distention, elevated liver enzymes, hepatomegaly, hiccups, increased appetite, melena, nausea, pancreatitis, peptic ulcer, ulcerative esophagitis, vomiting
GU: Amenorrhea, glycosuria, menstrual irregularities, perineal burning or tingling
HEME: Easy bruising, leukocytosis
MS: Arthralgia; aseptic necrosis of femoral and humeral heads; Charcot-like arthropathy; compression fractures; muscle atrophy, twitching, or weakness; myalgia; osteoporosis; spontaneous fractures; steroid myopathy; tendon rupture
RESP: Pulmonary edema
SKIN: Acne; allergic dermatitis; altered skin pigmentation; diaphoresis; dry, scaly skin; erythema; hirsutism; necrotizing vasculitis; petechiae; purpura; rash; scarring; sterile abscess; striae; subcutaneous fat atrophy; thin, fragile skin; urticaria
Other: Activation of latent infections, anaphylaxis, angioedema, exacerbation of systemic fungal infections, hypernatremia, hypocalcemia, hypokalemia, hypokalemic alkalosis, impaired wound healing, masking of signs of infection, metabolic alkalosis, suppressed skin test reaction, weight gain

Cautions

Use cautiously in patients with congestive heart failure or renal insufficiency because sodium retention and edema can occur in patients taking a corticosteroid. Also use cautiously in patients with peptic ulcer, diverticulitis, fresh intestinal anastomoses, or nonspecific ulcerative colitis; these conditions increase risk of perforation during corticosteroid therapy.

Give methylprednisolone tablets with food to minimize indigestion and GI irritation. For once-daily dosing, give in the morning to coincide with normal cortisol secretion. Expect prescriber to add an antacid or H2receptor antagonist to regimen.

Discard parenteral products that are discolored or contain particles. Discard any remaining Depo-Medrol suspension after prescribed dose is drawn from vial.

Inject I.M. form deep into gluteal muscle. Avoid injecting into deltoid muscle because of risk of subcutaneous atrophy.

Arrange for low-sodium diet with added potassium, as prescribed.

Protect patient from falling, especially elderly patient at risk for fractures from osteoporosis.

Closely monitor patient for signs of infection because drug may mask them or may worsen systemic fungal infections or active latent disease. Be aware that chickenpox and measles can become life-threatening in patients taking a corticosteroid.

Assess for possible depression or psychotic episodes during therapy.

Monitor blood glucose level; dosage of insulin or oral antidiabetic drug may need to be adjusted in diabetic patient.
WARNING To avoid possibly fatal acute adrenocortical insufficiency, expect to taper long-term therapy when discontinuing it, but expect dosage to be increased during times of stress.

Be aware that changes in thyroid function such as development of hypothyroidism or hyperthyroidism may require dosage adjustment in chronic therapy because metabolic clearance of methylprednisolone is affected by thyroid activity.

Avoid skin testing during methylprednisolone therapy because drug may suppress reaction.

PATIENT SAFTY

Caution patient not to stop taking methylprednisolone abruptly or to change dosage without consulting prescriber.

Tell patient to take a missed dose as soon as he remembers unless it’s nearly time for the next dose. Caution against doubledosing.

Urge patient to notify prescriber immediately about dark or tarry stools; signs of impending adrenocortical insufficiency, such as anorexia, dizziness, fainting, fatigue, fever, joint pain, muscle weakness, or nausea; and sudden weight gain or swelling.

Instruct patient not to obtain vaccinations unless approved by prescriber.

Urge patient to take vitamin D, calcium supplements, or both if recommended by prescriber.

Inform patient that insomnia and restlessness usually resolve after 1 to 3 weeks.

Caution patient to avoid people with contagious diseases.

Explain the need for regular exercise or physical therapy to maintain muscle mass.

Advise patient to carry medical identification that documents his need for longterm corticosteroid therapy.

Category

Chemical class: Benzamide
Therapeutic class: Antiemetic, upper GI stimulant

Pregnancy category: B

Indications

To treat diabetic gastroparesis

ORALL

, CONCENTRATE, Adults and adolescents.10 mg 30 min before meals and at bedtime up to q.i.d. I.V.OR
I.M.INJECTION Adults and adolescents.10 mg t.i.d. or q.i.d. for severe symptoms; dosage adjusted as needed. To treat gastroesophageal reflux disease

ORALL

, CONCENTRATE, Adults and adolescents. 10 to 15 mg 30 min before meals and at bedtime. To prevent chemotherapy-induced vomiting
IV: Adults and adolescents. 3 mg/kg before chemotherapy and then 0.5 mg/kg/hr for 8 hr.
I.V.INJECTION Adults and adolescents. 1 to 2 mg/kg 30 min before chemotherapy and then repeated every 2 to 3 hr, as needed. Children. 1 mg/kg as a single dose, repeated in 1 hr. Maximum: 2 mg/kg. To prevent postoperative nausea and vomiting

IM

Adults and adolescents.10 to 20 mg near end of procedure.
DOSAGE ADJUSTMENT Reduced by half if creatinine clearance is less than 40 ml/min/ 1.73 m2.

Mechanism of Action

Antagonizes the inhibitory effect of dopamine on GI smooth muscle. This causes gastric contraction, which promotes gasmetoclopramide hydrochloride 662 tric emptying and peristalsis, thus reducing gastroesophageal reflux. Metoclopramide also blocks dopaminergic receptors in the chemoreceptor trigger zone, preventing nausea and vomiting. Route Onset Peak Duration P.O. 30–60 min Unknown 1–2 hr I.V. 1–3 min Unknown 1–2 hr I.M. 10–15 min Unknown 1–2 hr

Incompatibilities

Don’t administer metoclopramide through same I.V. line as calcium gluconate, cephalothin sodium, chloramphenicol sodium, cisplatin, erythromycin lactobionate, furosemide, methotrexate, penicillin G potassium, or sodium bicarbonate.

Contraindications

Concurrent use of butyrophenones, phenothiazines, or other that may cause extrapyramidal reactions; GI hemorrhage, mechanical obstruction, or perforation; hypersensitivity to metoclopramide or its components; pheochromocytoma; seizure disorders

Interactions

anticholinergics, opioid analgesics: Possibly decreased metoclopramide effects apomorphine: Possibly decreased antiemetic effect of apomorphine, possibly increased CNS depression bromocriptine, pergolide: Possibly decreased therapeutic effects of these
cimetidine: Possibly decreased absorption and therapeutic effects of cimetidine
CNS depressants: Possibly increased CNS depression cyclosporine: Increased cyclosporine level digoxin: Decreased gastric digoxin absorption levodopa: Possibly decreased levodopa effects
MAO inhibitors: Increased risk of severe hypertension if patient has essential hypertension
mexiletine: Possibly faster mexiletene absorption succinylcholine: Possibly prolonged therapeutic action of succinylcholine
alcohol use: Risk of excessive sedation

Side Efect

CNS: Agitation, anxiety, depression, dizziness, drowsiness, extrapyramidal reactions (motor restlessness, parkinsonism, tardive dyskinesia), fatigue, headache, insomnia, irritability, lassitude, neuroleptic malignant syndrome, panic reaction, restlessness
CV: AV block, fluid retention, heart failure, hypertension, hypotension, supraventricular tachycardia
EENT: Dry mouth
ENDO: Galactorrhea, gynecomastia
GI: Constipation, diarrhea, nausea
GU: Menstrual irregularities
HEME: Agranulocytosis
SKIN: Rash
Other: Restless leg syndrome

Cautions

Use metoclopramide cautiously in patients with hypertension because it may increase catecholamine levels.
WARNING Watch closely for tardive dyskinesia, especially in the elderly, women, and patients with diabetes, because this serious adverse effect is often irreversible even after therapy stops. Therapy lasting longer than 12 weeks isn’t recommended because risk of tardive dyskinesia increases the longer the patient takes metoclopramide. Risk also has been linked to total cumulative dose so prescriber must take this into account when setting dosage. At first sign of involuntary movements of face, tongue, or limbs, notify prescriber and expect to discontinue drug.

Monitor patient with NADH-cytochrome b5 reductase deficiency because metoclopramide increases risk of methemoglobinemia and sulfhemoglobinemia, and patient can’t receive methylene blue.

Assess patient for signs of intestinal obstruction, such as abnormal bowel sounds, diarrhea, nausea, and vomiting, before administering metoclopramide. Notify prescriber if you detect them.

For I.V. use, you need not dilute doses of 10 mg or less. Give drug over 1 to 2 minutes. For doses larger than 10 mg, dilute in 50 ml normal saline solution, half-normal (0.45) saline solution, D5W, or lactated Ringer’s solution and infuse over at least 15 minutes.

Avoid rapid I.V. delivery because it may cause anxiety, restlessness, and drowsiness. metoclopramide hydrochloride 663 M
WARNING Notify prescriber if patient shows signs of toxicity, such as disorientation, drowsiness, and extrapyramidal reactions.

Monitor patient, especially one with heart failure or cirrhosis, for possible fluid retention or volume overload due to transient increase in plasma aldosterone level.

Monitor patient closely for neuroleptic malignant syndrome, a rare but potentially fatal disorder characterized by hyperthermia, muscle rigidity, altered level of consciousness, irregular pulse or blood pressure, tachycardia, diaphoresis, and arrhythmias.

Store drug in a light-resistant container; discard if discolored or contains particulate.

PATIENT SAFTY

Advise against activities that require alertness for about 2 hours after each dose.

Urge patient to avoid alcohol and CNS depressants while taking metoclopramide. They may increase CNS depression.

Tell patient to immediately report involuntary movements of face, eyes, tongue, or hands, including lip smacking, chewing, puckering of mouth, frowning, scowling, sticking out tongue, blinking, moving eyes, or shaking arms and legs.

Explain that stopping metoclopramide may cause withdrawal symptoms that include dizziness, nervousness, and headache.

Category

Chemical class: Quinazoline derivative
Therapeutic class: Antihypertensive, diuretic

Pregnancy category: B

Indications

To manage mild to moderate hypertension EXTENDED
Adults. 2.5 to 5 mg daily. PROMPT (MYKROX)
Adults. 0.5 mg daily. Maintenance: 0.5 to 1 mg daily. Maximum: 1 mg daily. To manage edema from heart failure or renal disease EXTENDED
Adults.5 to 20 mg daily.

Mechanism of Action

Promotes renal excretion of water and sodium by inhibiting their reabsorption in distal convoluted tubules. The resulting reduction in plasma and extracellular fluid volume reduces blood pressure. Metolazone also helps reduce blood pressure by decreasing peripheral vascular resistance. Route Onset Peak Duration P.O. 1 hr 2 hr 12–24 hr

Contraindications

Anuria; hepatic coma; hypersensitivity to metolazone, other sulfonamide derivatives, quinethazones, thiazides, or their components; renal failure

Interactions

allopurinol: Increased risk of hypersensitivity to allopurinol amiodarone: Increased risk of arrhythmias from hypokalemia amphotericin B: Increased risk of electrolyte imbalances anesthetics: Increased effects of anesthetics antigout : Increased blood uric acid level and risk of gout attack antihypertensives: Increased hypotension antineoplastics: Prolonged antineoplasticinduced leukopenia calcium salts: Increased risk of hypercalcemia cholestyramine, colestipol: Decreased metolazone absorption diazoxide: Increased risk of hyperglycemia digoxin: Increased risk of electrolyte imbalances and digoxin-induced arrhythmias diuretics: Additive effects of both , possibly leading to severe hypovolemia and electrolyte imbalances dopamine: Increased diuretic effect insulin, oral antidiabetic : Decreased effectiveness of these , increased risk of hyperglycemia lithium: Increased risk of lithium toxicity methenamine: Decreased metolazone effectiveness from urinary alkalinization methyldopa: Possibly hemolytic anemia neuromuscular blockers: Increased risk of hypokalemia and neuromuscular blockade, increased risk of respiratory depression NSAIDs, sympathomimetics: Possibly decreased metolazone effectiveness metozalone 664 oral anticoagulants: Decreased anticoagulation
vitamin D: Increased vitamin D action, increased risk of hypercalcemia

Side Efect

CNS: Anxiety, chills, depression, dizziness, drowsiness, headache, insomnia, neuropathy, paresthesia, restlessness, syncope, weakness
CV: Chest pain, cold extremities, orthostatic hypotension, palpitations, peripheral edema, vasculitis, venous thrombosis
EENT: Bitter taste, blurred vision, dry mouth, epistaxis, pharyngitis, sinus congestion, tinnitus
ENDO: Hyperglycemia
GI: Abdominal pain, anorexia, cholecystitis, constipation, diarrhea, hepatic dysfunction, hepatitis, indigestion, nausea, pancreatitis, vomiting
GU: Decreased libido, glycosuria, impotence
HEME: Agranulocytosis, aplastic anemia, leukopenia, thrombocytopenia
MS: Arthralgia, gout, myalgia
RESP: Cough
SKIN: Dry skin, necrosis, petechiae, photosensitivity, pruritus, rash, urticaria
Other: Hypochloremia, hypokalemia, hyponatremia, hypovolemia, metabolic alkalosis

Cautions

WARNING Be aware that Mykrox prompt tablets shouldn’t be substituted for Diulo or Zaroxolyn extended tablets because they aren’t equivalent.

Anticipate giving metolazone with a loop diuretic if patient responds poorly to loop diuretic alone.

To monitor drug’s diuretic effect, measure fluid intake and output and daily weight.

If response to 1 mg of Mykrox is inadequate, expect to add another drug rather than increase dosage.

Monitor blood chemistry test results and assess for evidence of hypochloremia, hypokalemia, and, possibly, mild metabolic alkalosis.

Monitor serum calcium and uric acid levels, especially if patient has a history of gout or renal calculi. Metolazone may slightly increase calcium reabsorption and decrease uric acid excretion.

PATIENT SAFTY

Inform patient that metolazone controls but doesn’t cure hypertension. Discuss possible need for lifelong therapy and consequences of uncontrolled hypertension.

Instruct patient to take drug at the same time each day.

Direct patient to take drug with food or milk to minimize adverse GI reactions.

Advise patient to change position slowly to minimize orthostatic hypotension.

Urge patient to notify prescriber about persistent, severe diarrhea, nausea, or vomiting, which can cause dehydration and orthostatic hypotension.

Stress the importance of weight and diet control, especially limiting sodium intake.

Inform diabetic patient that metolazone may increase blood glucose level and that he should check his level often.

Category

Chemical class: Beta1-adrenergic antagonist
Therapeutic class: Antianginal, antihypertensive, MI prophylaxis and treatment

Pregnancy category: C

Indications

To manage hypertension, alone or with other antihypertensives
Adults. Initial: 25 to 100 mg daily, adjusted weekly as prescribed. Maximum: 400 mg daily.
Adults.Maintenance: 100 to 400 mg daily to maintain blood pressure control after therapeutic level has been achieved with immediate-release tablets.
Adults. Initial: 100 mg daily, adjusted weekly as prescribed. Maximum: 450 mg daily as a single dose or in divided doses. To treat acute MI or evolving acute MI ,
I.V.INJECTION
Adults. Initial: 5 mg by I.V. bolus every 2 min for 3 doses followed by 50 mg P.O. for patients who tolerate total I.V. dose (25 to 50 mg P.O. for patients who can’t tolerate total I.V. dose) every 6 hr for 48 hr, starting 15 min after final I.V. dose; after 48 hr, 100 mg b.i.d. followed by maintenance dosage. Maintenance: 100 mg P.O. b.i.d. for at least 3 mo. To treat angina pectoris and chronic stable angina
Adults. 100 mg daily, increased weekly as prescribed. Maximum: 400 mg daily as a single dose or in divided doses.
Adults. Initial: 100 mg daily, adjusted weekly as prescribed. Maximum: 450 mg daily.
Adults. Initial: 50 mg b.i.d., adjusted weekly as prescribed. Maximum: 450 mg daily. To treat stable, symptomatic, ischemic, hypertensive, or cardiomyopathic heart failure
Adults. Initial: 25 mg daily (NYHA Class II) or 12.5 mg daily (NYHA Class III or more severe heart failure) for 2 wk. Then dosage doubled every 2 wk as tolerated. Maximum: 200 mg daily. Route Onset Peak Duration P.O. 60 min 1–2 hr Unknown P.O. () Unknown 6–12 hr Unknown I.V. Unknown 20 min Unknown

Mechanism of Action

Inhibits stimulation of beta1-receptor sites, located mainly in the heart, resulting in decreased cardiac excitability, cardiac output, and myocardial oxygen demand. These effects help relieve angina. Metoprolol also helps reduce blood pressure by decreasing renal release of renin.

Contraindications

Acute heart failure; pulse less than 45 beats/ minute; cardiogenic shock; hypersensitivity to metoprolol, its components, or other beta blockers; pheochromocytoma; secondor third-degree AV block; severe peripheral arterial disorders; sick sinus syndrome

Interactions

aluminum salts, barbiturates, calcium salts, cholestyramine, colestipol, NSAIDs, rifampin, salicylates, sulfinpyrazone: Decreased therapeutic effects of metoprolol amiodarone, digoxin, diltiazem, verapamil: Increased risk of complete AV block calcium channel blockers: Increased risk of heart failure and increased effects of both
cimetidine: Increased metoprolol level
clonidine: Increased risk of hypotension; increased risk of rebound hypertension when clonidine is discontinued digoxin: Decreased heart rate and slowed atrioventricular conduction estrogens: Possibly decreased antihypertensive effect of metoprolol general anesthetics: Increased risk of hypotension and heart failure insulin, oral antidiabetic : Decreased blood glucose control, possibly masking of signs and symptoms of hypoglycemia (by metoprolol) lidocaine: Increased risk of lidocaine toxicity
MAO inhibitors: Risk of hypertension neuromuscular blockers: Possibly enhanced and prolonged neuromuscular blockade other antihypertensives: Additive hypotensive effect phenothiazines: Possibly increased blood levels of both propafenone: Increased blood level and halflife of metoprolol sympathomimetics, xanthines: Possibly decreased therapeutic effects of both all : Increased bioavailability of metoprolol

Side Efect

CNS: Anxiety, confusion, depression, dizziness, drowsiness, fatigue, hallucinations, headache, insomnia, weakness
CV: Angina, arrhythmias (including AV block and bradycardia), chest pain, decreased HDL level, increased triglyceride levels, gangrene of extremity, heart failure, hypertension, orthostatic hypotension
EENT: Nasal congestion, rhinitis, taste disturbance
GI: Constipation, diarrhea, hepatitis, nausea, vomiting
GU: Impotence
HEME: Leukopenia, thrombocytopenia
MS: Arthralgia, back pain, myalgia
RESP: Bronchospasm, dyspnea
SKIN: Diaphoresis, photosensitivity, rash, urticaria, worsening of psoriasis

Cautions

Use metoprolol with extreme caution in patients with bronchospastic disease who don’t respond to or can’t tolerate other antihypertensives. Expect to give smaller doses more often to avoid the higher plasma levels in longer dosage intervals.

Use cautiously in patients with hypertension or angina who have congestive heart failure because beta blockers such as metoprolol can further depress myocardial contractility, worsening heart failure.

For patient with acute MI who can’t tolerate initial dosage or who delays treatment, start with maintenance dosage, as prescribed and tolerated.

Before starting therapy for heart failure, expect to give a diuretic, an ACE inhibitor, and digoxin to stabilize patient.

If patient has pheochromocytoma, alpha blocker therapy should start first, followed by metoprolol to prevent paradoxical increase in blood pressure from attenuation of beta-mediated vasodilation in skeletal muscle.

Be aware that metoprolol dosage for heart failure is highly individualized. Monitor patient for evidence of worsening heart failure during dosage increases. If heart failure worsens, expect to increase diuretic dosage and possibly decrease metoprolol dosage or temporarily discontinue drug, as prescribed. Metoprolol dosage shouldn’t be increased until worsening heart failure has been stabilized.

If patient with heart failure develops symptomatic bradycardia, expect to decrease the metoprolol dosage.
WARNING If dosage exceeds 400 mg daily, monitor patient for bronchospasm and dyspnea because metoprolol competitively blocks beta2-adrenergic receptors in bronchial and vascular smooth muscles.
WARNING When substituting metoprolol for clonidine, expect to gradually reduce clonidine and increase metoprolol dosage over several days. Given together, these have additive hypotensive effects.

Patients who take metoprolol may be at risk for AV block. If AV block results from depressed AV node conduction, prepare to give appropriate drug, as ordered, or assist with insertion of temporary pacemaker.

Check for signs of poor glucose control in patient with diabetes mellitus. Metoprolol may interfere with therapeutic effects of insulin and oral antidiabetic . It also may mask evidence of hypoglycemia, such as palpitations, tachycardia, and tremor.

Monitor patient with peripheral vascular disease for evidence of arterial insufficiency (pain, pallor, and coldness in affected extremity) Metoprolol can precipitate or aggravate peripheral vascular disease.
WARNING Expect to taper dosage over 1 to 2 weeks when drug is discontinued; stopping abruptly can cause myocardial ischemia, MI, ventricular arrhythmias, or severe hypertension, especially in patients with cardiac disease. Abrupt withdrawal also may cause thyroid storm in a patient with hyperthyroidism or thyrotoxicosis.

PATIENT SAFTY

Instruct patient to take metoprolol with food at the same time each day—once daily for tablets. Explain that he may halve tablets but not chew or crush them.

Advise patient to notify prescriber if pulse rate falls below 60 beats/minute or is significantly lower than usual.

Urge diabetic patient to check blood glucose level often during therapy.

Caution patient not to stop drug abruptly.

Category

Chemical class: Nitroimidazole derivative
Therapeutic class: Antibiotic, antiprotozoal

Pregnancy category: B

Indications

To treat systemic anaerobic infections caused by Bacteroides fragilis, Clostridium difficile, Clostridium perfringens, Eubacterium, Fusobacterium, Peptococcus, Peptostreptococcus, and Veillonella species , Adults and adolescents. 7.5 mg/kg up to 1,000 mg every 6 hr for 7 days or longer. Maximum: 4,000 mg daily. Children.7.5 mg/kg every 6 hr or 10 mg/kg every 8 hr.
IV: Adults and adolescents. Initial: 15 mg/kg and then 7.5 mg/kg up to 1,000 mg every 6 hr for 7 days or longer. Maximum: 4,000 mg daily. Children.7.5 mg/kg every 6 hr or 10 mg/kg every 8 hr. To treat amebiasis (Entamoeba histolytica) ,
Adults.500 to 750 mg t.i.d. for 5 to 10 days. Children. 11.6 to 16.7 mg/kg t.i.d. for 10 days. To treat trichomoniasis (Trichomonas vaginalis) ,
Adults. 2,000 mg as a single dose, 1,000 mg b.i.d. for 24 hr, or 250 mg t.i.d. for 7 days. Children.5 mg/kg t.i.d. for 7 days. To prevent perioperative bowel infection
IV: Adults and adolescents.15 mg/kg 1 hr before surgery and then 7.5 mg/kg 6 and 12 hr after initial dose. To treat acne in patients with rosacea TOPICAL GEL
Adults.Thin film applied to affected area b.i.d. for 9 wk. To treat bacterial vaginosis VAGINAL CREAM
Adults.500 mg (1 applicatorful) once or twice daily for 10 to 20 days. VAGINAL GEL
Adults. 37.5 mg (1 applicatorful) once or twice daily for 5 days. VAGINAL
Adults. 500 mg at bedtime for 10 to 20 days.

Mechanism of Action

Undergoes intracellular chemical reduction during anaerobic metabolism. After metronidazole is reduced, it damages DNA’s helical structure and breaks its strands, which inhibits bacterial nucleic acid synthesis and causes cell death.

Incompatibilities

Don’t administer I.V. metronidazole with aluminum needles or hubs or through same I.V. line as other .

Contraindications

Breast-feeding, hypersensitivity to metronidazole or its components, trichomoniasis during first trimester of pregnancy

Interactions

cimetidine: Possibly delayed elimination and increased blood level of metronidazole disulfiram: Possibly combined toxicity, with confusion and psychotic reactions neurotoxic : Increased risk of neurotoxicity oral anticoagulants: Possibly increased anticoagulant effect phenobarbital: Increased metabolism and decreased blood level and half-life of metronidazole
phenytoin: Decreased phenytoin clearance
alcohol use: Possibly disulfiram-like effects

Side Efect

CNS: Aseptic meningitis (parenteral form), ataxia, confusion, dizziness, encephalopathy, fever, headache, incoordination, insomnia, irritability, light-headedness, peripheral neuropathy, seizures (high doses), syncope, weakness, vertigo
EENT: Dry mouth, lacrimation (topical form), metallic taste, nasal congestion, optic neuropathy, pharyngitis
GI: Abdominal cramps or pain, anorexia, diarrhea, nausea, pancreatitis, vomiting
GU: Dark urine, vaginal candidiasis (oral, parenteral, and topical forms); burning or irritation of sexual partner’s penis, candidal cervicitis or vaginitis, dysuria, dryness of vagina or vulva, urinary frequency, vulvitis (vaginal form)
HEME: Leukopenia
MS: Back pain, dysarthria
SKIN: Burning or stinging sensation, dry skin (topical form); erythema, flushing, pruritus, rash, Stevens Johnson syndrome, urticaria (oral and parenteral forms)
Other: Injection site edema, pain, or tenderness

Cautions

Give I.V. drug by slow infusion over 1 hour; don’t give by direct I.V. injection.

Discontinue primary I.V. infusion during metronidazole infusion.
WARNING If patient has adverse CNS reactions, such as seizures or peripheral neuropathy, tell prescriber and stop drug immediately.

Monitor patient with severe liver disease because slowed metronidazole metabolism may cause drug to accumulate in body and increase the risk of adverse effects.

If skin irritation occurs, apply topical metronidazole gel less frequently or discontinue it, as ordered.

Monitor CBC and culture and sensitivity tests if therapy lasts longer than 10 days or if second course of treatment is needed.

PATIENT SAFTY

Instruct female patient to notify prescriber if she is pregnant, intends to get pregnant, or is breast-feeding.

Urge patient to take metronidazole at evenly spaced intervals day and with food to minimize adverse GI reactions.

Urge patient to complete the entire course of therapy.

Caution patient to avoid alcohol during therapy and for at least 3 days afterward.

Advise patient to avoid hazardous activities until drug’s CNS effects are known and to report any abnormal neurologic signs or symptoms, such as weakness, numbness, seizures, or vision changes.

If patient reports dry mouth, suggest ice chips or sugarless hard candy or gum; suggest a dental visit if dryness lasts longer than 2 weeks.

Instruct patient to notify prescriber if no improvement occurs within a few days of taking tablets or capsules.

Direct patient using topical gel to wash hands and affected area with a mild, nonirritating cleaner; to rinse well and pat dry; and then to apply a thin film of drug and wash hands again.

Advise patient with rosacea to keep topical gel away from his eyes. If drug gets into his eyes, urge him to wash them immediately with large amounts of cool tap water and to call prescriber if eyes continue to hurt or burn.

Instruct patient with rosacea to notify prescriber if no improvement occurs after 3 weeks of topical use; full therapeutic effect may take 9 weeks.

Teach patient how to fill, insert, and clean vaginal cream or gel applicator after use. Instruct her to wash her hands before and after administration.

To help vaginal tablets dissolve, instruct patient to run tap water over unwrapped tablet for a few seconds before insertion.

Inform patient with trichomoniasis that her male sexual partners should wear condoms during her treatment and that they may need treatment themselves to prevent reinfection.

Caution patient that vaginal cream and tablets (not gel) may contain oils that damage latex condoms.

Urge patient to follow up with prescriber to make sure infection is gone.

Category

Chemical class: Alpha-methyl tyrosine
Therapeutic class: Antipheochromocytoma agent

Pregnancy category: C

Indications

To control hypertension and related symptoms until pheochromocytomectomy is performed, to treat chronic malignant pheochromocytoma Adults and adolescents.Initial: 250 mg q.i.d., increased as ordered by 250 to 500 mg daily. Maintenance: 2,000 to 3,000 mg daily in divided doses q.i.d. Preoperative dosage given for at least 7 days. Maximum: 4,000 mg daily in divided doses.

Mechanism of Action

Blocks activity of tyrosine hydroxylase, the enzyme that controls rate of catecholamine synthesis. This action decreases production of the catecholamines epinephrine and norepinephrine, which, in patients with pheochromocytoma, are produced in excessive amounts.

Contraindications

Hypersensitivity to metyrosine or its components

Interactions

CNS depressants: Increased sedation haloperidol, phenothiazines: Increased extrapyramidal effects
alcohol use: Increased sedation

Side Efect

CNS: Anxiety, confusion, depression, disorientation, extrapyramidal reactions (difficulty speaking, drooling, parkinsonism, tremor, trismus), hallucinations, headache, sedation
CV: Peripheral edema
EENT: Dry mouth, nasal congestion, pharyngeal edema
ENDO: Galactorrhea, gynecomastia
GI: Abdominal pain, diarrhea, elevated serum AST level, nausea, vomiting
GU: Crystalluria, dysuria (transient), ejaculation failure, hematuria, impotence, urolithiasis
HEME: Anemia, eosinophilia, thrombocytopenia, thrombocytosis
SKIN: Urticaria

Cautions

Expect patient taking metyrosine to experience moderate to severe sedation at low and high dosages. Sedation begins during first 24 hours, peaks after 2 to 3 days, and tends to wane during next few days. It usually subsides after 1 week unless dosage is increased or exceeds 2 g daily.

Obtain urine specimens as ordered to check for crystalluria and urolithiasis. If crystalluria develops, increase fluid intake to achieve daily urine output of 2,000 ml or more with doses above 2 g daily. If crystalluria persists, reduce dosage or stop drug, as ordered.

Expect to adjust dosage, as prescribed, based on clinical response and urine catecholamine level.

If signs and symptoms aren’t adequately controlled by metyrosine, expect to add an alpha-adrenergic blocker, such as phenoxybenzamine, as prescribed.

PATIENT SAFTY

Inform patient about metyrosine’s sedative effects. Advise him to avoid alcohol and CNS depressants, which may increase sedation.

Instruct patient to increase fluid intake, as appropriate.

Urge patient to report drooling, severe diarrhea, trembling and shaking of hands and fingers, or trouble speaking.

Inform patient that he may experience changes in sleep pattern for 2 to 3 days after stopping drug.

Advise patient to keep regular visits with prescriber to monitor progress.

Category

Chemical class: Lidocaine analogue
Therapeutic class: Class IB antiarrhythmic

Pregnancy category: C

Indications

To treat life-threatening ventricular arrhythmias
Adults. Initial: 200 mg every 8 hr, adjusted, as ordered, by 50 to 100 mg/dose every 2 to 3 days, as tolerated. If patient tolerates 300 mg or less every 8 hr, total dosage may be divided and given every 12 hr. If patient continues to experience arrhythmias, dosage frequency may be changed to q.i.d. Maximum: 1,200 mg daily when given every 8 hr (400 mg/dose); 900 mg daily when given every 12 hr (450 mg/dose). To rapidly control life-threatening ventricular arrhythmias
Adults.Initial: 400 mg followed by 200 mg after 8 hr. Maintenance: 200 mg every 8 hr, adjusted, as ordered, by 50 to 100 mg/dose every 2 to 3 days, as tolerated. If patient tolerates 300 mg or less every 8 hr, total dosage may be divided and given every 12 hr. If patient continues to experience arrhythmias, dosage frequency may be changed to q.i.d.
DOSAGE ADJUSTMENT For patients with severe hepatic disease or heart failure, dosage reduced and adjusted every 2 or 3 days. Route Onset Peak Duration P.O. 0.5–2 hr 2–3 hr 8–12 hr

Mechanism of Action

Produces antiarrhythmic effect by inhibiting fast sodium channels in myocardial cell membranes, especially in the His-Purkinje system. This action decreases duration of action potential and effective refractory period of His-Purkinje system. The myocardium, which becomes refractory again after resting membrane potential is restored, is less likely to generate and respond to ectopic ventricular impulses.

Contraindications

Cardiogenic shock, secondor third-degree AV block without a pacemaker

Interactions

aluminumor magnesium-containing antacids: Delayed mexiletine absorption antiarrhythmics: Increased cardiac effects
cimetidine: Possibly increased or decreased blood mexiletine level hepatic enzyme inducers: Accelerated metabolism and decreased level of mexiletine metoclopramide: Accelerated mexiletine absorption
rifampin: Decreased blood mexiletine level
theophylline: Increased theophylline level urine acidifiers: Accelerated renal excretion of mexiletine urine alkalinizers: Delayed mexiletine excretion caffeine: Possibly decreased clearance and increased effects of caffeine that may acidify urine (such as cheese, cranberries, eggs, fish, grains, meats, plums, poultry, and prunes): Accelerated renal excretion of mexiletine that may alkalinize urine (such as milk and all vegetables and fruits except cranberries, plums, and prunes): Delayed renal excretion of mexiletine smoking: Reduced mexiletine half-life

Side Efect

CNS: Confusion, dizziness, fatigue, headache, lack of coordination, light-headedness, nervousness, paresthesia, seizures, sleep disturbance, syncope, tremor, weakness
CV: Atrial arrhythmias, AV conduction disorders, bradycardia, cardiogenic shock, chest pain, heart failure, hypotension, palpitations, PVCs, ventricular arrhythmias (increased)
EENT: Blurred vision, dry mouth, tinnitus
GI: Constipation, diarrhea, heartburn, nausea, vomiting HEME:Agranulocytosis, leukopenia, thrombocytopenia
RESP: Dyspnea
SKIN: Rash

Cautions

If mexiletine is replacing another antiarrhythmic, expect to give first dose 6 to 12 hours after last dose of quinidine sulfate or disopyramide, 3 to 6 hours after last dose of procainamide, or 8 to 12 hours after last dose of tocainide, as prescribed.

If mexiletine is replacing parenteral lidocaine, expect to reduce or withdraw lidocaine 1 to 2 hours after starting mexiletine, as prescribed.

Monitor continuous ECG and serum mexiletine level.

Assess patient for thrombocytopenia, which may occur within a few days after mexiletine therapy starts. Expect platelet count to return to normal within 1 month after mexiletine therapy stops.

PATIENT SAFTY

Instruct patient to take mexiletine at evenly spaced intervals, to avoid missing doses, and to take drug as prescribed, even if he’s feeling well.

Advise patient to take drug with food to reduce adverse GI reactions.

Inform patient that nausea and vomiting may occur within 2 hours after dose but tend to lessen as treatment continues.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Teach patient to take his pulse, and advise him to contact prescriber if rate is below 50 beats/minute or rhythm is irregular.

Urge patient to notify prescriber immediately about chest pain, chills, fast or irregular heartbeat, fever, shortness of breath, and unusual bleeding or bruising.

Advise patient to avoid greatly increasing intake of that may acidify urine (cheese, cranberries, eggs, fish, grains, meats, plums, poultry, prunes) or alkalinize urine (milk, all vegetables, all fruits except cranberries, plums, and prunes).

Encourage patient to keep regular visits with prescriber to monitor progress.

Category

Chemical class: Acyclaminopenicillin
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat moderate to severe infections, including bacteremia, bone and joint infections, gynecologic infections (such as endometritis, pelvic cellulitis, and pelvic inflammatory disease), intraabdominal infections (such as cholangitis, cholecystitis, hepatic abscess, intraabdominal abscess, and peritonitis), lower respiratory tract infections (such as pneumonia and lung abscess), meningitis, septicemia caused by susceptible bacteria, or skin and soft-tissue infections (such as cellulitis and diabetic foot ulcer); to manage febrile neutropenia
IV:,
I.M.INJECTION Adults and adolescents.3 g every 4 hr or 4 g every 6 hr. To treat life-threatening infections of the types listed above
IV:,
I.M.INJECTION Adults and adolescents. Up to 350 mg/kg daily. Maximum: 24,000 mg daily. Children and infants. 50 mg/kg every 4 hr (or infused over 30 min every 4 hr). Neonates over age 7 days weighing 2,000 g (4.4 lb) or less. 75 mg/kg I.V. every 8 hr. Neonates age 7 days or less weighing 2,000 g or less. 75 mg/kg I.V. every 12 hr. Neonates age 7 days or less weighing more than 2,000 g. 75 mg/kg I.V. every 6 hr. To treat uncomplicated UTI
IV:,
I.M.INJECTION
Adults.1.5 to 2 g every 6 hr. To treat complicated UTI
IV:
Adults. 3 g every 6 hr.
DOSAGE ADJUSTMENT Dosing interval extended to 6 to 8 hr if needed for patients with creatinine clearance of 10 to 30 ml/ min/1.73 m2. Dosing interval extended and dosage reduced to 1.5 to 2 g for patients with creatinine clearance below 10 ml/ min/1.73 m2. To treat uncomplicated gonorrhea caused by susceptible strains of Neisseria gonorrhoeae
IV:,
I.M.INJECTION
Adults.1 to 2 g as a single dose given with 1 g of probenecid P.O. (or probenecid given up to 30 min before mezlocillin). To prevent infection from potentially contaminated surgical procedures
IV:
Adults. 4 g 30 min before surgery and then 4 g every 6 hr for 2 more doses. To prevent infection in cesarean section
IV:
Adults. 4 g as soon as umbilical cord is clamped; then 4 g every 4 hr for 2 more doses, starting 4 hr after initial dose.

Mechanism of Action

Inhibits bacterial cell wall synthesis. In susceptible bacteria, the rigid, cross-linked cell wall is assembled in several stages. Mezlocillin affects final stage of cross-linking process by binding with and inactivating penicillin-binding proteins (enzymes responsible for linking cell wall strands). This causes bacterial cell lysis and death.

Incompatibilities

Administer mezlocillin at separate sites and at least 1 hour before or after administering aminoglycosides. Don’t mix mezlocillin in the same I.V. bag, bottle, or tubing with other .

Contraindications

Hypersensitivity to mezlocillin, other penicillins, or their components

Interactions

aminoglycosides: Substantial aminoglycoside inactivation chloramphenicol, erythromycins, sulfonamides, tetracyclines: Possibly decreased therapeutic effects of mezlocillin methotrexate: Increased risk of methotrexate toxicity probenecid: Increased blood level and prolonged half-life of mezlocillin

Side Efect

CNS: Depression, headache, seizures
EENT: Oral candidiasis
GI: Abdominal pain, diarrhea, pseudomembranous colitis, nausea, vomiting
GU: Vaginitis
HEME: Leukopenia, neutropenia
SKIN: Exfoliative dermatitis, pruritus, rash, urticaria
Other: Anaphylaxis; hypokalemia; injection site pain, redness, and swelling; serum sicknesslike reaction

Cautions

WARNING Before starting mezlocillin, make sure patient has had no previous hypersensitivity reactions to penicillins.

Anticipate that mezlocillin therapy will last for at least 2 days after signs and symptoms have resolved—typically 7 to 10 days, depending on severity of infection. Complicated infections may need longer treatment. Group A beta-hemolytic streptococcal infections usually are treated for at least 10 days to reduce risk of rheumatic fever or glomerulonephritis.

For I.M. injection, reconstitute each gram of mezlocillin with 3 to 4 ml sterile water for injection and shake vigorously. Inject no more than 2 g into a large muscle, such as the gluteus maximus, over 12 to 15 seconds to minimize discomfort.

Although drug may be given I.M., expect to use intermittent I.V. infusion, as directed, for serious infections.

For I.V. use, reconstitute each gram of mezlocillin with 9 to 10 ml sterile water for injection, D5W, or sodium chloride for injection and shake vigorously. Inject directly into I.V. tubing over 3 to 5 minutes.

For intermittent infusion, further dilute to desired volume (50 to 100 ml) with an appropriate I.V. solution and administer over 30 minutes. Discontinue other infusions during mezlocillin administration.

Be aware that mezlocillin powder and reconstituted solution may darken slightly but that potency isn’t affected.

Periodically monitor serum potassium level during long-term therapy, as ordered.

During long-term therapy, watch for signs and symptoms of superinfection, such as oral candidiasis and vaginitis.

PATIENT SAFTY

Instruct patient taking mezlocillin to notify prescriber immediately about increased bruising or other bleeding tendencies.

Advise patient to report diarrhea and to check with prescriber before taking an antidiarrheal medicine because of the risk of masking pseudomembranous colitis.

Category

Chemical class: Semisynthetic lipopeptide echinocandin
Therapeutic class: Antifungal

Pregnancy category: C

Indications

To treat esophageal candidiasis
IV:
Adults.150 mg infused over 1 hr daily. To prevent Candida infection in patients undergoing hematopoietic stem cell transplantation
IV:
Adults. 50 mg infused over 1 hr daily. To treat candidemia, acute disseminated candidiasis, and Candida peritonitis and abscesses
IV:
Adults. 100 mg infused over 1 hr daily.

Mechanism of Action

Inhibits synthesis of 1,3-beta-D-glucan, which is an essential component of the Candida fungal cell wall. Without 1,3-betaD-glucan, the fungal cell dies.

Contraindications

Hypersensitivity to micafungin, its components, or other echinocandins

Incompatibilities

Mixing or infusing with other may cause micafungin to precipitate.

Interactions

immunosuppressants: Possibly additive adverse hematologic effects itraconazole, nifedipine, sirolimus: Increased plasma levels of these

Side Efect

CNS: Anxiety, delirium, dizziness, dysgeusia, fatigue, fever, headache, insomnia, intracranial hemorrhage, rigors, seizures, somnolence
CV: Arrhythmia, atrial fibrillation, bradycardia, cardiac arrest, deep venous thrombosis, hypertension, hypotension, MI, peripheral edema, phlebitis, tachycardia, shock, vasodilation
EENT: Epistaxis, mucosal inflammation
ENDO: Hypoglycemia, hyperglycemia
GI: Abdominal pain, anorexia, constipation, diarrhea, dyspepsia, elevated liver enzyme levels, hepatic dysfunction, hiccups, hyperbilirubinemia, jaundice, nausea, vomiting
GU: Acute renal failure, anuria, elevated serum creatinine and blood urea levels, oliguria, renal tubular necrosis
HEME: Anemia, coagulopathy, eosinophilia, hemolytic anemia, leukopenia, lymphopenia, neutropenia, pancytopenia, thrombocytopenia
MS: Arthralgia, back pain
RESP: Apnea, cough, cyanosis, dyspnea, hypoxia, pneumonia, pulmonary embolism
SKIN: Erythema, erythema multiforme, flushing, necrosis, pruritus, rash, urticaria
Other: Acidosis, anaphylaxis, angioedema, bacteremia, hyperkalemia, hypernatremia, hypocalcemia, hypokalemia, hypomagnesemia, hyponatremia, hypophosphatemia, injection site reactions including phlebitis and thrombophlebitis, sepsis

Cautions

Use cautiously in patients with hepatic or renal insufficiency.

Reconstitute micafungin by adding 5 ml normal saline solution to each 50-mg vial being used (to yield 10 mg micafungin/ ml) or 5 ml normal saline solution to each 100-mg vial (to yield 20 mg micafungin/ ml). Swirl vial gently to minimize excessive foaming. Add reconstituted solution to 100 ml normal saline solution, and give solution over 1 hour. Protect diluted solution from light, although you need not cover the infusion drip chamber or tubing.

Always flush an existing intravenous line with normal saline solution before administering micafungin through that line.

Monitor infusion rate carefully because infusions that took less than 1 hour to infuse have been associated with more frequent hypersensitivity reactions.
WARNING Monitor patient closely for hypersensitivity reactions including anaphylaxis and angioedema. Stop infusion immediately if present, notify prescriber, and provide supportive care, as prescribed.

Monitor patient’s liver and renal function closely throughout therapy because liver and renal abnormalities may occur in patients receiving micafungin.

Monitor hematologic status closely because hematologic abnormalities may occur. If they do, monitor patient closely. If patient’s condition worsens, expect micafungin to be discontinued.

PATIENT SAFTY

Instruct patient to report any infusion site discomfort immediately.

Tell patient to report any unusual or persistent signs and symptoms to prescriber.

Category

Chemical class: Benzodiazepine
Therapeutic class: Sedative-hypnotic

Pregnancy category: D

Controlled substance schedule: IV

Indications

To induce preoperative sedation or amnesia, to control preoperative anxiety

ORALL

Children ages 6 months to 16 years. 0.25 to 0.5 mg/kg as a single dose 30 to 45 min before surgery. Usual: 0.5 mg/kg. Maximum: 20 mg.
I.V.INJECTION Adults age 60 and over. 1.5 mg over 2 min immediately before procedure. After 2-min waiting period, dosage adjusted to desired level in 25% increments, as ordered. Maximum: 1 mg in 2 min. Adults under age 60 and adolescents.Up to 2.5 mg over 2 min immediately before procedure. After 2-min waiting period, dosage adjusted to desired level in 25% increments, as ordered. Maximum: 5 mg. Children ages 6 to 12. Initial: 0.025 to 0.05 mg/kg, up to 0.4 mg/kg, if needed. Maximum: 10 mg. Children ages 6 months to 5 years. Initial: 0.05 to 0.1 mg/kg, up to 0.6 mg/kg, if needed. Maximum: 6 mg.

IM

Adults age 60 and over. 0.02 to 0.05 mg/kg as a single dose 30 to 60 min before surgery. Adults under age 60 and adolescents. 0.07 to 0.08 mg/kg as a single dose 30 to 60 min before surgery. Children ages 6 months to 12 years. 0.1 to 0.15 mg/kg, up to 0.5 mg/kg for more anxious patients. Maximum: 10 mg. To relieve agitation and anxiety in mechanically ventilated patients
IV:
Adults. Initial: 0.01 to 0.05 mg/kg infused over several min, repeated at 10to 15-min intervals until adequate sedation occurs. Maintenance: 0.02 to 0.1 mg/kg/hr initially, adjusted to desired level in 25% to 50% increments, as ordered. After achieving desired level of sedation, infusion rate decreased by 10% to 25% every few hr, as ordered, until minimum effective infusion rate is determined. Children. Initial: 50 to 200 mcg/kg over 2 to 3 min followed by 1 to 2 mcg/kg/min by continuous infusion. Maintenance: 0.4 to 6 mcg/kg/min. Infants over age 32 weeks. 1 mcg/kg/min by continuous infusion. Infants under age 32 weeks.0.5 mcg/kg/ min by continuous infusion. Route Onset Peak Duration I.V.* 1.5–5 min Rapid 2–6 hr I.M.* 5–15 min 15–60 min 2–6 hr I.M. 30–60 Unknown Unknown min

Mechanism of Action

May exert sedating effect by increasing activity of gamma-aminobutyric acid, a major inhibitory neurotransmitter in the brain. As a result, midazolam produces a calming effect, relaxes skeletal muscles, and—at high doses—induces sleep.

Contraindications

Acute angle-closure glaucoma; alcohol intoxication; coma; hypersensitivity to midazolam, other benzodiazepines, or their components; shock

Interactions

antihypertensives: Increased risk of hypotension cimetidine, diltiazem, erythromycin, fluconazole, indinavir, itraconazole, ketoconazole, ranitidine, ritonavir, saquinavir, verapamil: Intense and prolonged sedation caused by reduced midazolam metabolism
CNS depressants: Possibly increased CNS and respiratory depression and hypotension
rifampin: Decreased blood midazolam level grapefruit, grapefruit juice: Possibly increased blood midazolam level and risk of toxicity
alcohol use: Possibly intense, prolonged sedative effect and increased respiratory depression and hypotension

Side Efect

CNS: Agitation, delirium, or dreaming during emergence from anesthesia; anxiety; ataxia; chills; combativeness; confusion; dizziness; drowsiness; euphoria; excessive sedation; headache; insomnia; lethargy; nervousness; nightmares; paresthesia; prolonged emergence from anesthesia; restlessness; retrograde amnesia; sleep disturbance; slurred speech; weakness; yawning
CV: Cardiac arrest, hypotension, nodal rhythm, PVCs, tachycardia, vasovagal episodes
EENT: Blurred vision, diplopia, or other vision changes; increased salivation; laryngospasm; miosis; nystagmus; toothache
GI: Hiccups, nausea, retching, vomiting
RESP: Airway obstruction, bradypnea, bronchospasm, coughing, decreased tidal volume, dyspnea, hyperventilation, respiratory arrest, shallow breathing, tachypnea, wheezing
SKIN: Pruritus, rash, urticaria
Other: Injection site burning, edema, induration, pain, redness, and tenderness

Cautions

Before giving midazolam, determine whether patient consumes alcohol or takes midazolam hydrochloride 675 M * For sedation. For amnesia. antihypertensives, antibiotics, or protease inhibitors because these substances can produce an intense and prolonged sedative effect when taken with midazolam.
WARNING I.V. midazolam is given only in hospital or ambulatory care settings that allow continuous monitoring of respiratory and cardiac function. Keep resuscitative and equipment at hand.

As needed, combine midazolam injection with D5W, normal saline solution, or lactated Ringer’s solution. With D5W and normal saline, solution is stable 24 hours. With lactated Ringer’s, solution is stable 4 hours.

As needed, mix injection in same syringe with atropine sulfate, meperidine hydrochloride, morphine sulfate, or scopolamine hydrobromide. The resulting solution is stable for 30 minutes.

Assess level of consciousness frequently because the range between sedation and unconsciousness or disorientation is narrow with midazolam.

Be aware that recovery time is usually 2 hours but may be up to 6 hours.

PATIENT SAFTY

Inform patient that he may not remember procedure because midazolam produces amnesia.

Advise patient to avoid hazardous activities until drug’s adverse CNS effects, such as dizziness and drowsiness, have worn off.

Instruct patient to avoid alcohol and other CNS depressants for 24 hours after receiving drug, as directed by prescriber.

Category

Chemical class: Desglymidodrine prodrug
Therapeutic class: Antihypotensive, vasopressor

Pregnancy category: C

Indications

To treat symptomatic orthostatic hypotension
Adults. 10 mg t.i.d. in 3to 4-hr intervals.
DOSAGE ADJUSTMENT Initial dose possibly reduced to 2.5 mg for patients with renal impairment. Route Onset Peak Duration P.O. Unknown 30 min 2–3 hr

Mechanism of Action

Is broken down into the active metabolite desglymidodrine. Desglymidodrine directly stimulates alpha-adrenergic receptors in arteries and veins. This action increases total peripheral vascular resistance, which in turn increases systolic and diastolic blood pressure.

Contraindications

Acute renal disease, hypersensitivity to midodrine or its components, initial supine systolic pressure above 180 mm Hg, persistent and excessive supine hypertension, pheo-chromocytoma, severe heart disease, thyrotoxicosis, urine retention

Interactions

beta blockers, digoxin: Enhanced or precipitated bradycardia, AV block, arrhythmias cimetidine, flecainide, metformin, procainamide, quinidine, ranitidine, triamterene: Possibly decreased renal clearance of these dihydroergotamine, ephedrine, phenylephrine, phenylpropanolamine, pseudoephedrine: Increased vasopressor effects doxazosin, prazosin, terazosin: Antagonized midodrine effects fludrocortisone acetate: Increased risk of supine hypertension

Side Efect

CNS: Anxiety, asthenia, chills, confusion, delusions, dizziness, feeling of pressure or fullness in head, headache, hyperesthesia, insomnia, nervousness, paresthesia, somnolence
CV: Hypertension (sitting and supine), vasodilation
EENT: Canker sore, dry mouth, vision changes
GI: Flatulence, indigestion, nausea
GU: Dysuria, urinary frequency and urgency, urine retention
MS: Back pain, leg cramps
SKIN: Dry skin, erythema multiforme, facial flushing, piloerection, rash, scalp pruritus

Cautions

Monitor hepatic and renal function, as ordered, before and during midodrine therapy.

Give drug at 3to 4-hour intervals, if ordered and needed to control symptoms. Don’t give after evening meal, less than 4 hours before bed, or more often than every 3 hours.
WARNING Monitor for severe, persistent systolic supine hypertension, which may develop with single doses up to 20 mg.

Avoid placing patient flat in bed for any length of time. Elevate head of bed when patient is supine.

Monitor supine and sitting blood pressure often during midodrine therapy.

PATIENT SAFTY

Instruct patient to take midodrine every 3 to 4 hours during daytime but not to take final dose after evening meal or within 4 hours of going to bed.

Advise patient to elevate head of bed when he lies supine. Caution him not to remain flat for any length of time.

Direct patient to notify prescriber immediately about headache, increased dizziness, urine retention, or vision changes.

Encourage patient to keep follow-up appointments to monitor blood pressure and hepatic and renal function.

Category

Chemical class: Desoxynojirimycin derivative
Therapeutic class: Alpha-glucosidase inhibitor, antidiabetic drug

Pregnancy category: B

Indications

To manage type 2 diabetes mellitus
Adults. Initial: 25 mg t.i.d. with first bite of each meal. Or, 25 mg daily, increased gradually to 25 mg t.i.d. Maximum: 100 mg t.i.d.
DOSAGE ADJUSTMENT After 4 to 8 wk, dosage increased, if ordered, to 50 mg t.i.d. for about 3 mo; then dosage adjusted based on glycosylated hemoglobin (HbA1C) level. Route Onset Peak Duration P.O. Rapid 2–3 hr Unknown

Mechanism of Action

Inhibits intestinal glucoside hydrolase enzymes, which normally hydrolyze oligosaccharides and disaccharides to glucose and other monosaccharides. This action delays carbohydrate digestion and absorption and reduces postprandial blood glucose level.

Contraindications

Acute or chronic bowel disorder, diabetic ketoacidosis, hypersensitivity to miglitol or its components

Interactions

digestive enzyme preparations, intestinal adsorbents (activated charcoal): Decreased miglitol effects digoxin: Decreased blood digoxin level propranolol, ranitidine: Decreased bioavailability of these

Side Efect

GI: Abdominal pain, diarrhea, flatulence, hepatotoxicity
HEME: Low serum iron level
SKIN: Rash (transient)

Cautions

Use miglitol cautiously in patient with serum creatinine level above 2 mg/dl.

Be aware that some patients with type 2 diabetes also may receive a sulfonylurea as an adjunct to miglitol therapy.

Give miglitol with first bite of each meal. Drug must have arrived at site of enzymatic action when carbohydrates reach small intestine.

Review patient’s HbA1Clevel, as appropriate, to monitor long-term glucose control.

Monitor patient for evidence of overdose, such as transient increases in abdominal discomfort, diarrhea, and flatulence (but not hypoglycemia).

PATIENT SAFTY

Explain that miglitol is an adjunct to diet, which is the primary treatment for type 2 diabetes mellitus.

Instruct patient to take drug with first bite of each meal.

Describe signs and symptoms of hypoglycemia and pathophysiology of diabetes to patient and family members.

If miglitol is the only drug patient takes to control blood glucose level, explain that it won’t cause hypoglycemia.

If patient takes a sulfonylurea or insulin with miglitol,recommend that he keep a source of glucose readily available to reverse hypoglycemia.

Explain importance of monitoring blood and urine glucose levels.

Explain that adverse GI reactions usually decrease in frequency and intensity over time.

Teach obese patient about weight loss, calorie restriction, diet, and regular exercise, as indicated.

Category

Chemical class: Selective norepinephrine and serotonin reuptake inhibitor
Therapeutic class: Anti-fibromyalgia

Pregnancy category: C

Indications

To manage fibromyalgia Adults and adolescents age 17 and over. Initial: 12.5 mg on day one; 12.5 mg b.i.d. on days 2 and 3; 25 mg b.i.d. on days 4 through 7; and then 50 mg b.i.d., increased, if needed to 100 mg b.i.d. Maximum: 100 mg b.i.d.
DOSAGE ADJUSTMENT For patients with severe renal impairment (creatinine clearance of 5 to 29 ml/min/1.73 m2), maintenance dosage reduced by half. Route Onset Peak Duration P.O. Unknown 2–4 hr Unknown

Mechanism of Action

Inhibits reuptake of norepinephrine and serotonin by CNS neurons without affecting uptake of dopamine or other neurotransmitters, thereby increasing amount of norepinephrine and serotonin available in nerve synapses. Elevated norepinephrine and serotonin levels may improve symptoms of fibromyalgia, including by central analgesic effect.

Contraindications

Hypersensitivity to milnacipran or its components, uncontrolled narrow-angle glaucoma, use within 14 days of MAO inhibitor

Interactions

aspirin, NSAIDs,
warfarin: Increased risk of bleeding clomipramine: Increased risk of euphoria and postural hypotension
clonidine: Possibly inhibited antihypertensive effect CNS-active : Possibly increased CNS effects digoxin (I.V.): Possibly increased risk of postural hypotension and tachycardia epinephrine, norepinephrine: Increased risk of arrhythmias and paroxysmal hypertension lithium: Increased risk of serotonin syndrome
MAO inhibitors: Possibly hyperpyretic episodes, hypertensive crisis, serotonin syndrome, and severe seizures serotonergic such as SSRIs, triptans, and
tramadol: Incrased risk of hypertension and coronary artery vasoconstriction
alcohol use: Increased risk of liver impairment

Side Efect

CNS: Anxiety, chills, delirium, depression, dizziness, fatigue, fever, hallucinations, headache, hypoesthesia, insomnia, irritability, loss of consciousness, migraine, neuroleptic malignant sydrome, parkinsonism, paresthesia, seizures, serotonin syndrome, suicidal ideation, tremor
CV: Chest pain, hypercholesterolemia, hypertension, hypertensive crisis, increased heart rate, palpitations, peripheral edema, somnolence, supraventricular tachycardia, tachycardia
EENT: Accommodation abnormality, blurred vision, dry mouth, mydriasis
ENDO: Hot flashes, hyperprolactinemia
GI: Abdominal distention or pain, anorexia, constipation, diarrhea, dyspepsia, elevated liver enzymes, gastroesophageal reflux, flatulence, hepatitis, jaundice, liver dysfunction, nausea, vomiting
GU: Acute renal failure, cystitis, decreased libido, dysuria, ejaculation disorder, erectile dysfunction, prostatitis, scrotal or testicular pain, testicular swelling, urinary hesitation, urine retention, urethral pain, UTI
HEME: Leukeopenia, neutropenia, thrombocytopenia
MS: Rhabdomyolysis
RESP: Dyspnea, upper respiratory infection
SKIN: Erythema multiforme, flushing, hyperhidrosis, night sweats, pruritus, rash, Stevens-Johnson syndrome
Other: Hyponatremia, weight gain or loss

Cautions

Because milnacipran may aggravate liver disease, it shouldn’t be given to patients with alcohol addiction or chronic liver disease.

Use cautiously in patients with mild to moderate renal impairment and patients with significant hypertension or cardiac disease. Also use cautiously in patients with a history of dysuria, especially men with prostatic hypertrophy, prostatitis, and other lower urinary tract obstructive disorders.

At least 14 days should elapse between stopping an MAO inhibitor and starting milnacipran. At least 5 days should elapse between stopping milnacipran and starting an MAO inhibitor.

Measure patient’s blood pressure and heart rate before starting and periodically during milnacipran therapy because drug can raise blood pressure and heart rate. If hypertension or tachycardia occurs and persists, notify prescriber and expect to reduce dosage or discontinue drug.

Watch closely for suicidal tendencies, especially when therapy starts and dosage changes.
WARNING Monitor patient closely for serotonin syndrome, a rare but serious adverse effect of selective serotonin reuptake inhibitors such as milnacipran. Signs and symptoms include agitation, confusion, diaphoresis, diarrhea, fever, hyperactive reflexes, poor coordination, restlessness, shaking, talking or acting with uncontrolled excitement, tremor, and twitching. If symptoms occur, notify prescriber immediately, expect to discontinue drug, and provide supportive care.

Monitor patient’s liver function. If jaundice or signs and symptoms of liver dysfunction occur, notify prescriber and expect drug to be discontinued.

Watch for hypersensitivity reactions, especially in patients with aspirin sensitivity, because drug contains the yellow dye tartrazine.

Check patient’s serum sodium level, as ordered, because drug may cause hyponatremia, especially in elderly patients, patients taking diuretics, and patients who are volume depleted.

Expect to taper drug when no longer needed, as ordered, to minimize adverse reactions.

PATIENT SAFTY

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes.

Caution patient against stopping drug abruptly because serious adverse effects may result.

Instruct patient to alert all prescribers that he takes milnacipran.

Tell patient to have his blood pressure monitored regularly throughout milnacipran therapy.

Advise patient to avoid activities, such as driving, that require alertness until the CNS effects of milnacipran are known.

Caution patient to avoid aspirin and NSAIDs, if possible, while taking milnacipran.

Category

Chemical class: Bipyridine derivative
Therapeutic class: Inotropic, vasodilator

Pregnancy category: C

Indications

To provide short-term treatment of acute heart failure
IV:
Adults. Loading: 50 mcg/kg over 10 min (at milrinone lactate 679 M least 0.375 mcg/kg/min). Usual: 0.375 to 0.75 mcg/kg/min. Maximum: 1.13 mg/kg daily.
DOSAGE ADJUSTMENT Dosage adjusted according to cardiac output, pulmonary artery wedge pressure (PAWP), and clinical response. If creatinine clearance is 30 to 39 ml/min/1.73 m2, infusion rate reduced to 0.33 mcg/kg/min; if 20 to 29 ml/min/ 1.73 m2, to 0.28 mcg/kg/min; if 10 to 19 ml/min/1.73 m2, to 0.23 mcg/kg/min; and if less than 9 ml/min/1.73 m2, to 0.2 mcg/kg/min. Route Onset Peak Duration I.V. 5–15 min Unknown 3–6 hr

Incompatibilities

Don’t administer milrinone through same I.V. line as furosemide because precipitate will form. Don’t add other to premixed milrinone flexible containers.

Contraindications

Hypersensitivity to milrinone or its components

Interactions

antihypertensives: Possibly hypotension

Side Efect

CNS: Headache, tremor
CV: Angina, hypotension, supraventricular arrhythmias, ventricular ectopic activity, ventricular fibrillation, ventricular tachycardia, torsades de pointes
GI: Liver function test abnormalities
HEME: Thrombocytopenia
RESP: Bronchospasm
SKIN: Rash
Other: Anaphylactic shock, hypokalemia, infusion site reactions (pain, swelling, redness)

Cautions

Make sure ECG equipment is available for continuous monitoring during milrinone therapy.

Discard drug if it’s discolored or contains particles.

For loading dose, infuse undiluted drug directly into I.V. line with compatible infusing solution. For continuous infumilrinone lactate 680 Cell exterior Cell interior Cell exterior Blocked calcium movement Hormone receptor Degraded cAMP Myocardial cell membrane Cell interior cAMP Calcium movement into cell Phosphodiesterase inhibited by milrinone Phosphodiesterase Milrinone cAMP Cell exterior Cell interior Cell exterior Blocked calcium movement Hormone receptor Degraded cAMP Myocardial cell membrane Cell interior cAMP Calcium movement into cell Phosphodiesterase inhibited by Phosphodiesterase Milrinone cAMP

Mechanism of Action

An inotropic drug, milrinone increases the force of myocardial contraction—and cardiac output—by blocking the enzyme phosphodiesterase. Normally, this enzyme is activated by hormones binding to cell membrane receptors. As shown below left, phosphodiesterase normally degrades intracellular cAMP, which restricts calcium movement into myocardial cells. By inhibiting phosphodiesterase, as shown below right, milrinone slows the rate of cAMP degradation, increasing the intracellular cAMP level and the amount of calcium that enters myocardial cells. In blood vessels, increased cAMP causes smooth-muscle relaxation, which improves cardiac output by reducing preload and afterload. sion, dilute drug with half-normal (0.45) saline solution, normal saline solution, or D5W. Dilution isn’t needed when using premixed milrinone flexible containers.

Check platelet count before and periodically during infusion, as ordered. Expect to discontinue drug if platelet count falls below 150,000/mm3.

Give loading dose using a controlled-rate infusion device. For continuous infusion, use a calibrated electronic infusion device.

Monitor cardiac output, pulmonary artery wedge pressure, blood pressure, heart rate, weight, and fluid status during therapy to determine drug effectiveness.

Monitor renal and liver function test results and serum electrolyte levels. Notify prescriber of abnormalities.

If severe hypotension develops, notify prescriber at once and expect to stop drug.

Expect patient to receive digoxin before starting milrinone, which can increase ventricular response rate.

PATIENT SAFTY

Reassure patient that you will be present and that he will be monitored constantly during therapy.

Category

Chemical class: Tetracycline
Therapeutic class: Antibiotic, antiprotozoal

Pregnancy category: D

Indications

To treat bartonellosis, brucellosis, chancroid, granuloma inguinale, inclusion conjunctivitis, lymphogranuloma venereum, nongonococcal urethritis, plague, psittacosis, Q fever, relapsing fever, respiratory tract infections (including pneumonia), rickettsial pox, Rocky Mountain spotted fever, tularemia, typhus, and UTI caused by gramnegative organisms (including Bartonella bacilliformis, Brucella species, Haemophilus ducreyi, Haemophilus influenzae,Vibrio cholerae, and Yersinia pestis), susceptible gram-positive organisms (including certain strains of Streptococcus pneumoniae), and other organisms (including Actinomyces species, Bacillus anthracis, Borrelia recurrentis, Chlamydia species, Mycoplasma pneumoniae, and Rickettsiae); as adjunct to treat intestinal amebiasis and as alternative to treat listeriosis caused by Listeria monocytogenes, syphilis caused by Treponema pallidum, and yaws caused by Treponema pertenue for nonpregnant patients allergic to penicillin , ORAL SUSPENSION Adults and adolescents.Initial: 200 mg. Maintenance: 100 mg every 12 hr. Or 100 to 200 mg initially followed by 50 mg every 6 hr. Children over age 8. Initial: 4 mg/kg. Maintenance: 2 mg/kg every 12 hr.
I.V.INJECTION Adults and adolescents. Initial: 200 mg. Maintenance: 100 mg every 12 hr. Maximum: 400 mg daily. Children over age 8. Initial: 4 mg/kg. Maintenance: 2 mg/kg every 12 hr.
DOSAGE ADJUSTMENT If patient has renal impairment, don’t exceed 200 mg daily. As adjunct to treat inflammatory acne vulgaris that’s unresponsive to oral tetracycline or erythromycin , ORAL SUSPENSION Adults and adolescents. 50 mg once daily to t.i.d. To treat inflammatory lesions of nonnodular moderate to severe acne vulgaris Adults and adolescents. 1 mg/kg once daily for 12 weeks.
DOSAGE ADJUSTMENT For patient with renal impairment, dosage reduced or time interval between doses extended. To treat uncomplicated gonorrhea from Neisseria gonorrhoeae in nonpregnant patients allergic to penicillin , ORAL SUSPENSION Adults and adolescents. Initial: 200 mg. Maintenance: 100 mg every 12 hr for at least 4 days. To treat uncomplicated gonococcal urethritis in men , ORAL SUSPENSION Adults and adolescents. 100 mg b.i.d. for 5 days. To treat asymptomatic meningococcal carriers with Neisseria meningitidis in nasopharynx , ORAL SUSPENSION Adults and adolescents.100 mg every 12 hr for 5 days. Children over age 8. Initial: 4 mg/kg. Maintenance: 2 mg/kg every 12 hr for 5 days. To treat infections caused by Mycobacterium marinum , ORAL SUSPENSION
Adults. 100 mg every 12 hr for 6 to 8 wk. Route Onset Peak Duration P.O. Unknown 2–4 hr 6–12 hr I.V. Unknown Unknown 6–12 hr

Mechanism of Action

Inhibits bacterial protein synthesis by competitively binding to the 30S ribosomal subunit of the mRNA-ribosome complex of certain organisms.

Incompatibilities

Don’t mix minocycline in same syringe with solution that contains calcium because precipitate will form.

Contraindications

Hypersensitivity to minocycline, other tetracyclines, or their components

Interactions

aluminum-, calcium-, or magnesiumcontaining antacids; calcium supplements; choline and magnesium salicylates; ironcontaining preparations; magnesiumcontaining laxatives; sodium bicarbonate: Possibly formation of nonabsorbable complex, impaired minocycline absorption cholestyramine, colestipol: Possibly impaired cholestyramine or colestipol absorption
cimetidine: Possibly decreased GI absorption and effectiveness of minocycline digoxin: Possibly increased blood digoxin level and risk of digitalis toxicity insulin: Possibly decreased need for insulin iron salts: Possibly decreased GI absorption and antimicrobial effect of minocycline lithium: Possibly increased or decreased blood lithium level
methoxyflurane: Increased risk of nephrotoxicity oral anticoagulants: Possibly potentiated anticoagulant effects oral contraceptives containing estrogen: Decreased contraceptive effectiveness, increased risk of breakthrough bleeding penicillin: Interference with bactericidal action of penicillin vitamin A: Possibly benign intracranial hypertension

Side Efect

CNS: Dizziness, fever, headache, lightheadedness, unsteadiness, vertigo
CV: Pericarditis
EENT: Blurred vision, darkened or discolored tongue, glossitis, papilledema, tooth discoloration, vision changes
GI: Abdominal cramps or pain, anorexia, diarrhea, dysphagia, enterocolitis, esophageal irritation and ulceration, hepatitis, hepatotoxicity, indigestion, nausea, pancreatitis, pseudomembranous colitis, vomiting
GU: Genital candidiasis, nephrotoxicity
HEME: Eosinophilia, hemolytic anemia, neutropenia, thrombocytopenia, thrombocytopenic purpura
MS: Arthralgia, myopathy (transient)
RESP: Pulmonary infiltrates (with eosinophilia)
SKIN: Erythema multiforme, exfoliative dermatitis, brown pigmentation of skin and mucous membranes, erythematous and maculopapular rash, jaundice, onycholysis, photosensitivity, pruritus, purpura (anaphylactoid), Stevens-Johnson syndrome, urticaria
Other: Anaphylaxis, angioedema, serum sicknesslike reaction, systemic lupus erythematosus exacerbation

Cautions

Use minocycline cautiously in patients with renal or hepatic dysfunction and in those taking other hepatotoxic because drug may cause nephrotoxicity or hepatotoxicity.
WARNING Notify prescriber if patient is breast-feeding because drug appears in breast milk and may have toxic effects.

Monitor blood, renal, and hepatic tests before and during long-term therapy.

Shake oral suspension well before use.

To prepare drug for I.V. use, reconstitute each 100-mg vial with 5 to 10 ml sterile water for injection. Further dilute in 500 to 1,000 ml normal saline solution, D5W, dextrose 5% in normal saline solution, or Ringer’s or lactated Ringer’s solution. Administer final dilution immediately, but avoid rapid administration.

Store reconstituted drug at room temperature and use within 24 hours.

Assess patient for signs of superinfection; if they appear, notify prescriber, discontinue minocycline, and start appropriate therapy, as ordered.

Monitor patient for development of foul smelling diarrhea, which suggests Clostridium difficile. If present, notify prescriber, obtain stool culture, and expect to withhold minocycline and provide supportive care, as indicated and ordered.

Monitor PT in patient who also takes an anticoagulant during minocycline therapy.

PATIENT SAFTY

Instruct patient to shake oral suspension well and to use calibrated measuring device.

Advise patient to take minocycline with a full glass of water, with food or milk, and in an upright position to minimize esophageal and GI irritation.

Direct patient to take a missed dose as soon as he remembers unless it’s nearly time for the next dose. Caution against double-dosing.

Instruct patient not to take minocycline within 2 hours of an antacid or 3 hours of an iron preparation.

Urge patient to complete full course of treatment even if he feels better before finishing.

Instruct patient to notify prescriber if no improvement occurs in a few days.

Advise patient to avoid prolonged exposure to sun or sunlamps during therapy.

Counsel female patient to avoid becoming pregnant because minocycline should be avoided, if possible, during tooth development (last half of gestation up to age 8). Drug may permanently turn teeth yellow, gray, or brown and cause enamel hypoplasia. It also may slow skeletal growth and cause congenital anomalies, including limb reduction.

Encourage patient who uses an oral contraceptive to use additional contraceptive method during minocycline therapy.

Instruct patient to notify prescriber immediately about blurred vision, dizziness, headache, known or suspected pregnancy, and unsteadiness.

Explain that diarrhea may occur up to 2 months after completing therapy; urge patient to notify prescriber if it occurs.

Category

Chemical class: Piperidinopyrimidine derivative
Therapeutic class: Antihypertensive (oral), hair-growth stimulant (topical)

Pregnancy category: C

Indications

To manage severe symptomatic hypertension or hypertension with target organ damage that’s unresponsive to other treatment Adults and adolescents. Initial: 5 mg as a single dose or divided doses b.i.d. Increased, as directed, after at least 3 days. Maintenance: 10 to 40 mg daily. Maximum: 100 mg daily. Children. Initial: 0.2 mg/kg daily. Increased, as directed, after at least 3 days. Maintenance: 0.25 to 1 mg/kg daily as a single dose or in divided doses b.i.d. Maximum: 50-mg starting dose, 50 mg daily.
DOSAGE ADJUSTMENT Dosage possibly reduced for elderly patients and those who have renal failure or are having dialysis. To treat alopecia TOPICAL2% Adults up to age 65. 1 ml applied b.i.d. to area of desired hair growth. TOPICAL 5% Adult men up to age 65. 1 ml applied b.i.d. to area of desired hair growth. Route Onset Peak Duration P.O. 30 min 2–3 hr 24–48 hr Topical 2% 4 mo 1 yr Unknown Topical 5% 2 mo 1 yr Unknown

Mechanism of Action

Reduces blood pressure by inhibiting intracellular phosphodiesterase, an enzyme that facilitates hydrolysis of cAMP and cGMP. This action decreases the intracellular cAMP level, relaxes arterial smooth muscles, and lowers blood pressure. Oral minoxidil produces greater dilation in arteries than in veins. It also reduces peripheral resistance and increases heart rate, cardiac output, and stroke volume. Topical minoxidil may cause hair regrowth by increasing cutaneous blood flow and stimulating resting hair follicles.

Contraindications

Acute MI; dissecting aortic aneurysm; hypersensitivity to minoxidil or its components, including propylene glycol; pheochromocytoma; skin irritation or abrasions (topical)

Interactions

guanethidine: Possibly severe hypotension, increased risk of orthostatic hypotension (oral) nitrates, other hypotension-producing , potent parenteral antihypertensives: Possibly severe hypotension NSAIDs, sympathomimetics: Decreased antihypertensive effects topical petrolatum, topical steroids: Increased absorption of topical minoxidil if used on same area topical retinoids: Increased absorption of topical minoxidil and, possibly, formation of granulation tissue

Side Efect

CNS: Fatigue, paresthesia (oral); light-headedness, neuritis (topical); headache (both)
CV: ECG changes, heart failure, pericardial tamponade, pericarditis, rebound hypertension (oral); cardiac tamponade, hypotension, palpitations, reflex hypertension (topical); angina, edema, fast or irregular heartbeat, pericardial effusion (both)
EENT: Vision changes (topical)
ENDO: Breast tenderness (oral)
GI: Abdominal distention, ascites, nausea, vomiting (oral)
GU: Elevated BUN and serum creatinine levels (oral); sexual dysfunction (topical)
HEME: Leukopenia; thrombocytopenia; transient decrease in hematocrit, hemoglobin, and erythrocyte counts (oral)
RESP: Dyspnea, pulmonary hypertension (oral)
SKIN: Flushing, hyperpigmentation, Stevens-Johnson syndrome (oral); allergic contact dermatitis, alopecia, dry or flaky skin, eczema, erythema, folliculitis, scalp burning (topical); hypertrichosis, rash (both)
Other: Facial edema (topical); sodium and water retention, weight gain (both)

Cautions

WARNING Be aware that patient who receives guanethidine should be hospitalized before starting oral minoxidil therapy so that his blood pressure can be monitored.

Be aware that drug isn’t usually prescribed for mild hypertension.

For rapid management of hypertension, expect to adjust dosage up to every 6 hours and to monitor patient as prescribed. Also expect to give a beta blocker and diuretic.

Monitor progress by measuring blood pressure often and weight daily. Evaluate for signs of fluid and sodium retention and for other systemic

Side Efect

.

Watch for signs of pericardial effusion. Be prepared to stop oral minoxidil, if ordered.

Expect to discontinue oral minoxidil gradually because abrupt discontinuation may lead to rebound hypertension.

Apply topical drug only on healthy scalp. Avoid sunburned or abraded scalp.

Use gloves when applying solution.

Avoid inhaling mist from spray applicator.

Expect minoxidil to be least effective in men with mainly frontal hair loss.

Expect topical form to have little effect on blood pressure in patients who don’t have hypertension.

PATIENT SAFTY

Inform patient that oral minoxidil controls but doesn’t cure hypertension.

Advise him to take tablets at the same time every day.

Teach patient to take his radial pulse, and advise him to take it daily. Instruct him to notify prescriber if it exceeds normal rate by 20 beats/minute or more.

Stress the importance of daily blood pressure and weight measurements.

Instruct patient to notify prescriber immediately about bloating, breathing problems, a fast or irregular heartbeat, flushed or red skin, swelling of feet or lower legs, or weight gain of more than 5 lb (2.3 kg) in 1 day.

Advise patient to have regular checkups with prescriber to monitor progress.

Urge patient to consult prescriber before taking other prescription or OTC .

Reassure patient that body hair thickening and darkening reverses after oral minoxidil is discontinued.

For patient using topical minoxidil, teach proper application technique and provide manufacturer’s written instructions. Advise him to wear gloves when applying drug and to make sure hair and scalp are dry first.

Instruct patient to start applying drug at center of balding area, to let dry for 2 to 4 hours, and not to use hairdryer to help it dry faster.

Warn patient to avoid applying drug to abraded, irritated, or sunburned areas of scalp; to avoid inhaling mist when using a spray applicator; and to avoid getting drug in his eyes, nose, or mouth. If accidental contact does occur, advise him to flush the area with large amounts of cool tap water.

Instruct patient not to shampoo his hair for at least 4 hours after application and to avoid using other skin products on treated skin. Direct him to avoid using minoxidil for 24 hours before and after chemical hair products, such as dyes and relaxers.

Caution patient not to use more drug or apply it more often than prescribed and not to apply it to other body areas. Explain the risk of adverse systemic reactions with excessive topical use.

Tell patient to keep topical minoxidil away from heat or flame because it’s flammable.

Inform patient that minoxidil may stain clothing, hats, or bed linens before it’s dry.

Instruct patient to notify prescriber if burning, itching, or redness develops after application. For severe reactions, advise patient to wash drug off and consult prescriber before applying it again.

Urge patient to consult prescriber if hair loss continues after 2 weeks or if growth fails to increase in 4 months.

Inform patient that new hair growth may be lost 3 to 4 months after stopping topical minoxidil and that progressive hair loss will resume.

Category

Chemical class: Piperazinoazepine
Therapeutic class: Antidepressant

Pregnancy category: C

Indications

To treat major depression
,
Adults.Initial: 15 mg daily, preferably at bedtime. Increased as needed and tolerated at 1to 2-wk intervals. Maximum: 45 mg daily. Route Onset Peak Duration P.O. 1–2 wk 6 wk or Unknown longer

Mechanism of Action

May inhibit neuronal reuptake of norepinephrine and serotonin. By doing so, this tetracyclic antidepressant increases the action of these neurotransmitters in nerve cells. Increased neuronal serotonin and norepinephrine levels may elevate mood.

Contraindications

Hypersensitivity to mirtazapine or its components, use within 14 days of an MAO inhibitor

Interactions

antihypertensives: Increased hypotensive effects of these or enhanced mirtazapine effects anxiolytics, hypnotics, other CNS depressants (including sedatives): Increased CNS depression
MAO inhibitors: Possibly hyperpyrexia, hypertension, seizures
alcohol use: Increased CNS depression

Side Efect

CNS: Agitation, amnesia, anxiety, apathy, asthenia, ataxia, cerebral ischemia, chills, confusion, delirium, delusions, depersonalization, depression, dizziness, dream disturbances, drowsiness, dyskinesia, dystonia, emotional lability, euphoria, extrapyramidal reactions, fever, hallucinations, hostility, hyperkinesia, hyperreflexia, hypoesthesia, hypokinesia, lack of coordination, malaise, mania, migraine headache, neurosis, paranoia, paresthesia, seizures, somnolence, syncope, tremor, vertigo
CV: Angina, bradycardia, edema, hypercholesterolemia, hypertension, hypertriglyceridemia, hypotension, MI, orthostatic hypotension, peripheral edema, PVCs, vasodilation
EENT: Accommodation disturbances, conjunctivitis, dry mouth, earache, epistaxis, eye pain, glaucoma, gingival bleeding, glossitis, hearing loss, hyperacusis, keratoconjunctivitis, lacrimation, pharyngitis, sinusitis, stomatitis
ENDO: Breast pain
GI: Abdominal distention and pain, anorexia, cholecystitis, colitis, constipation, elevated ALT level, eructation, increased appetite, nausea, thirst, vomiting
GU: Amenorrhea, cystitis, dysmenorrhea, dysuria, hematuria, impotence, increased libido, leukorrhea, renal calculi, urinary frequency and incontinence, urine retention, UTI, vaginitis
HEME: Agranulocytosis, neutropenia
MS: Arthralgia, back pain, dysarthria, muscle twitching, myalgia, myasthenia, neck pain and rigidity
RESP: Asthma, bronchitis, cough, dyspnea, pneumonia
SKIN: Acne, alopecia, dry skin, exfoliative dermatitis, photosensitivity, pruritus, rash
Other: Dehydration, facial edema, flulike symptoms, herpes simplex, weight change

Cautions

Administer mirtazapine before bedtime.

Expect disintegrating tablet to dissolve on patient’s tongue within 30 seconds.
WARNING Don’t give drug within 14 days of an MAO inhibitor to avoid serious, possibly fatal, reaction.

If patient takes drug for depression, watch closely for suicidal tendencies, especially when therapy starts or dosage changes, because depression may briefly worsen.

Monitor patient closely for infection (fever, pharyngitis, stomatitis), which may be linked to a low WBC count. If these signs occur, notify prescriber and expect to stop drug.

Expect mirtazapine therapy to last 6 months or longer for acute depression.

PATIENT SAFTY

Instruct patient not to swallow disintegrating tablet. Tell him to hold tablet on tongue and let it dissolve. Inform him that tablet will dissolve within 30 seconds.

Inform phenylketonuric patient that mirtazapine
contain phenlyalanine 2.6 mg per 15-mg tablet, 5.2 mg per 30-mg tablet, and 7.8 mg per 45-mg tablet.

Instruct patient to avoid alcohol and other CNS depressants during therapy and for up to 7 days after drug is discontinued.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Direct patient to change position slowly to minimize the effects of orthostatic hypotension.

Instruct patient to notify prescriber at once about chills, fever, mouth irritation, sore throat, and other signs of infection.

Encourage patient to visit prescriber regularly during therapy to monitor progress.

Category

Chemical class: Prostaglandin E1analogue
Therapeutic class: Antiulcer, gastric antisecretory

Pregnancy category: X

Indications

To prevent NSAID-induced gastric ulcers
Adults. 200 mcg q.i.d. or 400 mcg b.i.d. misoprostol 686 with food, with last dose at bedtime every day.
DOSAGE ADJUSTMENT Dosage reduced to 100 mcg q.i.d. if patient can’t tolerate 200-mcg dose. Route Onset Peak Duration P.O. 30 min 60–90 min 3–6 hr

Mechanism of Action

May protect the stomach from NSAIDinduced mucosal damage by increasing gastric mucus production and mucosal bicarbonate secretion. Misoprostol also inhibits gastric acid secretion caused by such stimuli as food, coffee, and histamine.

Contraindications

Hypersensitivity to prostaglandins or their analogues, pregnancy

Interactions

magnesium-containing antacids: Increased misoprostol-induced diarrhea

Side Efect

CNS: Anxiety, asthenia, chills, confusion, depression, drowsiness, dizziness, fatigue, fever, headache, neuropathy, neurosis, rigors, stroke, syncope, thirst
CV: Arrhythmias, chest pain, edema, hypertension, hypotension, increased cardiac enzyme levels, MI, phlebitis, thromboembolism
EENT: Abnormal taste or vision, conjunctivitis, deafness, earache, epistaxis, gingivitis, tinnitus
ENDO: Hyperglycemia
GI: Abdominal pain, constipation, diarrhea, dysphagia, flatulence, GI bleeding or inflammation, hepatobiliary dysfunction, indigestion, nausea, reflux, vomiting
GU: Dysmenorrhea, dysuria, hematuria, hypermenorrhea, impotence, loss of libido, menstrual irregularities, polyuria, urinary tract infection, vaginal bleeding
HEME: Anemia, abnormal differential thrombocytopenia purpura, increased erythrocyte sedimentation rate
MS: Arthralgia, back pain, myalgia, muscle cramps or stiffness
RESP: Bronchitis, bronchospasm, dyspnea, pneumonia, pulmonary embolism, upper respiratory tract infection
SKIN: Alopecia, diaphoresis, dermatitis, pallor, rash
Other: Anaphylaxis, gout, weight changes

Cautions

WARNING Ask female patient if she is or may be pregnant. If so, notify prescriber because misoprostol may cause uterine bleeding, contractions, spontaneous abortion, and teratogenic effects in the fetus.

Use drug cautiously in patients with cerebrovascular disease, coronary artery disease, or uncontrolled epilepsy because of the risk of severe complications.

Also use misoprostol cautiously in patients with inflammatory bowel disease because drug may worsen intestinal inflammation and cause diarrhea. If diarrhea causes severe dehydration, misoprostol may be discontinued.

PATIENT SAFTY

Caution female patient about risk of taking misoprostol during pregnancy, and urge her to use reliable contraception during therapy. Urge her to notify prescriber at once if she is or might be pregnant.

Instruct patient to take misoprostol with meals and at bedtime.

Advise patient that he may take NSAIDs, if prescribed, during misoprostol therapy.

Explain that diarrhea is dose related and usually resolves after 8 days. Tell patient to avoid magnesium-containing antacids because they may worsen diarrhea and to call prescriber if diarrhea lasts more than 8 days.

Urge female patient to notify prescriber immediately about postmenopausal bleeding; she may need diagnostic tests.

Category

Chemical class: Anthracenedione
Therapeutic class: Antineoplastic

Pregnancy category: D

Indications

To reduce neurologic disability and frequency of relapses in patients with secmitoxantrone hydrochloride 687 M ondary (chronic) progressive, progressive relapsing, or worsening relapsingremitting multiple sclerosis (patients whose neurologic status is significantly abnormal between relapses)
IV:
Adults. 12 mg/m2over 5 to 15 min every 3 mo. Maximum: Cumulative dose of 140 mg/m2. As adjunct to treat pain related to advanced hormone-refractory prostate cancer
IV:
Adults. 12 to 14 mg/m2 over 5 to 15 min every 21 days. As adjunct to treat acute nonlymphocytic leukemia (ANLL)
IV:
Adults. Initial: 12 mg/m2over at least 3 min on days 1 to 3 with 100 mg/m2of cytarabine as a continuous 24-hr infusion on days 1 to 7. If patient’s antileukemic response is inadequate or incomplete, second induction course is given at same dosage. Maintenance: 6 wk after induction, 12 mg/m2over at least 3 min on days 1 and 2 with 100 mg/m2of cytarabine as a continuous 24-hr infusion on days 1 to 5. A second maintenance course is given 4 wk after the first if needed and tolerated.

Mechanism of Action

Binds to DNA, causing cross-linkage and strand breakage, interfering with RNA synthesis, and inhibiting topoisomerase II, an enzyme that uncoils and repairs damaged DNA. Mitoxantrone produces a cytocidal effect on proliferating and nonproliferating cells and doesn’t appear to be cell-cycle specific. It’s known to inhibit B-cell, T-cell, and macrophage proliferation and impair antigen function.

Incompatibilities

Don’t mix mitoxantrone in the same infusion as heparin (because a precipitate may form); don’t mix with any other .

Contraindications

Hypersensitivity to mitoxantrone or its components

Interactions

allopurinol, colchicine, probenecid, sulfinpyrazone: Possibly interference with antihyperuricemic action of these blood-dyscrasia–causing (such as cephalosporins and sulfasalazine): Increased risk of leukopenia and thrombocytopenia bone marrow depressants, such as carboplatin and lomustine: Possibly additive bone marrow depression daunorubicin, doxorubicin: Increased risk of cardiotoxicity methotrexate and other antineoplastics: Risk of developing leukemia vaccines, killed virus: Decreased antibody response to vaccine vaccines, live virus: Increased risk of replication of and adverse effects of vaccine virus, decreased antibody response to vaccine

Side Efect

CNS: Headache, seizures
CV: Arrhythmias, cardiotoxicity, chest pain, congestive heart failure, decreased left ventricular ejection fraction, ECG changes
EENT: Blue-colored cornea, conjunctivitis, mucositis, stomatitis
GI: Abdominal pain, diarrhea, GI bleeding, nausea, vomiting
GU: Blue-green urine, renal failure
HEME: Acute myelogenous leukemia, leukopenia, other leukemias, thrombocytopenia
MS: Myelodysplasia
RESP: Cough, dyspnea
SKIN: Alopecia, extravasation, jaundice
Other: Allergic reaction, anaphylaxis, hyperuricemia, infection, infusion site pain or redness

Cautions

Before mitoxantrone therapy and before each dose, expect patient to have an ECG and evaluation of left ventricular ejection fraction. Expect to obtain hematocrit, hemoglobin level, and CBC with platelet count. If patient’s left ventricular ejection fraction drops below normal, expect drug to be discontinued.

Be aware that drug shouldn’t be given to patient with multiple sclerosis whose neutrophil count is less than 1,500/mm3or who has a below-normal left ventricular ejection fraction.

Check liver function test results, as ordered, before each course of therapy. Expect that drug won’t be given to multiple sclerosis patient with abnormal liver function.

Assess patient for cardiac dysfunction throughout therapy. Watch for evidence of cardiotoxicity, such as arrhythmias and chest pain, in patient with heart disease. Risk increases when cumulative dose reaches 140 mg/m2in cancer or 100 mg/ m2in multiple sclerosis. Notify prescriber of any significant changes, and expect drug to be discontinued. Be aware that congestive heart failure may occur months or years after drug has been discontinued.

Anticipate obtaining pregnancy test before each course of therapy for women of childbearing age with multiple sclerosis.

Follow facility policy for handling antineoplastics. Be aware that manufacturer recommends goggles, gloves, and a gown during drug preparation and delivery.

Before infusing drug, dilute it in at least 50 ml of normal saline solution or D5W.
WARNING Drug shouldn’t be given intrathecally because paralysis may occur.

If mitoxantrone solution contacts your skin or mucosa, wash thoroughly with warm water. If it contacts your eyes, irrigate them thoroughly with water or normal saline solution.

Discard unused diluted solution because it contains no preservatives. After penetration of stopper, store undiluted drug for up to 7 days at room temperature or 14 days refrigerated. Avoid freezing drug.

If extravasation occurs, stop infusion immediately and notify prescriber. Reinsert I.V. line in another vein and resume infusion. Although mitoxantrone is a nonvesicant, observe the extravasation site for signs of necrosis or phlebitis.

Monitor patients with chickenpox or recent exposure and patients with herpes zoster for severe, generalized disease.

Monitor blood uric acid level for hyperuricemia in patients with a history of gout or renal calculi. Expect to give allopurinol, as prescribed, to patients with leukemia or lymphoma and elevated blood uric acid level to prevent uric acid nephropathy.
WARNING If severe or life-threatening nonhematologic or hematologic toxicity occurs during first induction course, expect to withhold the second course until it resolves.

If patient develops thrombocytopenia, take precautions per facility policy.

Assess patient for evidence of infection, such as fever, if leukopenia occurs. Expect to obtain appropriate specimens for culture and sensitivity testing.

Be aware that patients receiving mitoxantrone in combination with other antineoplastics or radiation therapy are at risk for developing secondary leukemia, including acute myelogenous leukemia.

PATIENT SAFTY

Advise patient to complete dental work, if possible, before treatment begins or defer it until blood counts return to normal; drug may delay healing and cause gingival bleeding. Teach patient proper oral hygiene, and advise use of a toothbrush with soft bristles.

Urge patient to drink plenty of fluid to increase urine output and uric acid excretion.

Advise patient to contact prescriber immediately if GI upset occurs, but to continue taking drug unless otherwise directed.

Stress the importance of complying with the dosage regimen and keeping follow-up medical and laboratory appointments.

Explain that urine may appear blue-green for 24 hours after treatment and that the whites of the eyes may appear blue. Stress that these effects are temporary and harmless. Explain that hair loss is possible, but that hair should return after therapy ends.

Caution patient not to receive immunizations unless approved by prescriber. Also, advise persons who live in same household as patient to avoid receiving immunization with oral polio vaccine. Tell patient to avoid persons who recently received the oral polio vaccine or to wear a mask over his nose and mouth.

Instruct patient to avoid persons with infections if bone marrow depression occurs. Advise patient to contact prescriber if fever, chills, cough, hoarseness, lower back or side pain, or painful or difficult urination occurs; these changes may signal an infection.

Tell patient to contact prescriber immediately if he has unusual bleeding or bruising, black or tarry stools, blood in urine or stool, or pinpoint red spots on his skin.

Urge patient not to touch his eyes or the inside of his nose unless he has just washed his hands.

Stress the need to avoid accidental cuts, as from a razor or fingernail clippers, because of possible excessive bleeding or infection.

Caution patient to avoid contact sports or activities that may cause bruising or injury.

Urge patient to comply with yearly examinations after therapy ends to check for late-occurring drug-induced heart problems. Tell patient to report trouble breathing, swelling in legs or ankles, or an uneven or fast heartbeat even after drug has been discontinued.

Category

Chemical class: Benzhydryl sulfinylacetamide derivative
Therapeutic class: CNS stimulant

Pregnancy category: C

Controlled substance schedule: IV

Indications

To improve daytime wakefulness in patients with narcolepsy, obstructive sleep apnea hypopnea syndrome, and shift work sleep disorder Adults and adolescents age 16 and over. 200 mg daily in the morning or 1 hr before starting work shift Maximum: 400 mg daily.
DOSAGE ADJUSTMENT For patients with severe hepatic impairment, dosage should be reduced by 50%.

Mechanism of Action

May inhibit the release of gamma-aminobutyric acid (GABA), the most common inhibitory neurotransmitter, or CNS depressant, in the brain. Modafinil also increases the release of glutamate, an excitatory neurotransmitter, or CNS stimulant, in the thalamus and hippocampus. These two actions may improve wakefulness.

Contraindications

Hypersensitivity to modafinil or its components

Interactions

amitriptyline, citalopram, clomipramine, diazepam, imipramine, propranolol, tolbutamide, topiramate: Possibly prolonged elimination time and increased blood levels of these carbamazepine: Possibly decreased modafinil effectiveness and decreased blood carbamazepine level cimetidine, clarithromycin, erythromycin, fluconazole, fluoxetine, fluvoxamine, itraconazole, ketoconazole, nefazodone, sertraline: Possibly inhibited metabolism, decreased clearance, and increased blood level of modafinil contraceptive-containing implants or devices, oral contraceptives: Possibly contraceptive failure cyclosporine: Possibly decreased blood cyclosporine level and increased risk of organ transplant rejection dexamethasone, phenobarbital and other barbiturates, primidone, rifabutin,
rifampin: Possibly decreased blood level and effectiveness of modafinil dextroamphetamine,
methylphenidate: Possibly 1-hour delay in modafinil absorption when these are given together fosphenytoin, mephenytoin,
phenytoin: Possibly decreased effectiveness of modafinil, increased blood phenytoin level, and increased risk of phenytoin toxicity
theophylline: Possibly decreased blood level and effectiveness of theophylline triazolam: Possibly decreased effectiveness of triazolam
warfarin: Possibly decreased warfarin metabolism and increased risk of bleeding all : 1-hour delay in modafinil absorption and possibly delayed onset of action caffeine: Increased CNS stimulation grapefruit juice: Possibly decreased modafinil metabolism

Side Efect

CNS: Aggressiveness, agitation, anxiety, confusion, delusions, depression, hallucinations, headache, insomnia, mania, nervousness, psychosis, suicidal ideation
GI: Nausea
HEME: Agranulocytosis
SKIN: Drug rash with eosinophilia and systemic symptoms (DRESS), rash, StevensJohnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, angioedema, infection, multi-organ hypersensitivity

Cautions

Modafinil shouldn’t be given to patients with mitral valve prolapse syndrome or a history of left ventricular hypertrophy because drug may cause ischemic changes.

Use cautiously in patients with recent MI or unstable angina because effect of drug is unknown in these disorders.

Use cautiously in patients with a history of psychosis, depression, or mania because these conditions may worsen during therapy and may require modafinil to be stopped.
WARNING Monitor patient with a history of alcoholism, stimulant abuse, or other substance abuse for compliance with modafinil therapy. Observe for signs of misuse or abuse, including frequent prescription refill requests, increased frequency of dosing, or drug-seeking behavior. Also watch for evidence of excessive modafinil dosage, including aggressiveness, anxiety, confusion, decreased prothrombin time, diarrhea, irritability, nausea, nervousness, palpitations, sleep disturbances, and tremor.

Be aware that modafinil, like other CNS stimulants, may alter mood, perception, thinking, judgment, feelings, motor skills, and signs that patient needs sleep.

If giving drug to patient with a history of psychosis, emotional instability, or psychological illness with psychotic features, be prepared to perform baseline behavioral assessments or frequent clinical observation.

Stop drug at first sign of rash, and notify prescriber. Although rare, rash may indicate a potentially life-threatening event.

Monitor patient for signs and symptoms of multisystem organ hypersensitivity, such as fever, rash, myocarditis, hepatitis, hematologic abnormalities, pruritus, asthenia, or any other serious abnormality because multi-organ hypersensitivity may vary in its presentation. Notify prescriber if suspected, and expect to discontinue drug and provide supportive care, as ordered.

Watch closely for suicidal tendencies, especially in patients with a psychiatric history.

PATIENT SAFTY

Inform patient that modafinil can help, but not cure, narcolepsy and that drug’s full effects may not be seen right away.

Advise patient to avoid taking modafinil within 1 hour of eating because food may delay drug’s absorption and onset of action. If he drinks grapefruit juice, encourage him to drink a consistent amount daily.

Instruct patient to stop taking modafinil and to notify precriber if he develops a rash, fever, or other serious effect.

Urge patient to report chest pain, depression, anxiety, or evidence of psychosis or mania to prescriber.

Inform patient that drug can affect concentration and function and can hide signs of fatigue. Urge him not to drive or perform activities that require mental alertness until full CNS effects are known.

Because alcohol may decrease alertness, advise patient to avoid it while taking modafinil.

Encourage a regular sleeping pattern.

Caution patient to avoid excessive intake of , beverages, and OTC that contain caffeine because caffeine may lead to increased CNS stimulation.

Inform female patient that modafinil can decrease the effectiveness of certain contraceptives, including birth control pills and implantable hormonal contraceptives. If she uses such contraceptives, urge her to use an alternate birth control method during modafinil therapy and for up to 1 month after she stops taking the drug.

Advise patient to keep follow-up appointments with prescriber so that her progress can be monitored.

Urge family or caregiver to watch patient closely for abnormal behaviors, including suicidal tendencies, especially if patient has a psychiatric history.

Category

Chemical class: Prodrug of moexiprilat
Therapeutic class: Antihypertensive

Pregnancy category: C

(first trimester), D (later trimesters)

Indications

To manage hypertension without diuretic therapy
Adults. Initial: 7.5 mg daily 1 hr before a meal. Maintenance: 7.5 to 30 mg as a single dose or in divided doses b.i.d. 1 hr before meals. Maximum: 30 mg/day.
DOSAGE ADJUSTMENT For patients with creatinine clearance of less than 40 ml/min/ 1.73 m2, initial dosage reduced to 3.75 mg daily and increased, as ordered, to maximum of 15 mg daily. To manage hypertension with diuretic therapy
Adults. Initial: 3.75 mg daily 1 hr before a meal. Increased gradually, as ordered, until blood pressure is controlled. Route Onset Peak Duration P.O. 1 hr 3–6 hr 24 hr

Mechanism of Action

Is converted to the active metabolite moexiprilat, which reduces blood pressure by inhibiting ACE activity. ACE normally catalyzes conversion of angiotensin I to angiotensin II—a vasoconstrictor that stimulates aldosterone secretion by adrenal cortex and directly suppresses renin release. Inhibited ACE activity results in decreased peripheral arterial resistance, increased plasma renin activity, and decreased aldosterone secretion. Decreased aldosterone secretion causes water and sodium excretion.

Contraindications

History of angioedema with previous ACE inhibitor use, hypersensitivity to moexipril or its components

Interactions

allopurinol, bone marrow depressants, corticosteroids (systemic), cytostatic , procainamide: Increased risk of possibly fatal neutropenia or agranulocytosis antacids: Possibly decreased moexipril bioavailability cyclosporine, heparin, potassium-containing , potassium-sparing diuretics, potassium supplements: Increased risk of hyperkalemia digoxin: Possibly increased digoxin level diuretics, other hypotension-producing : Hypotension, risk of renal failure (from sodium or volume depletion), possibly decreased secondary aldosteronism and hypokalemia caused by diuretics lithium: Increased blood lithium level and risk of lithium toxicity NSAIDs (especially indomethacin), sympathomimetics: Decreased antihypertensive effect of moexipril phenothiazines: Increased pharmacologic effects of moexipril all : Decreased moexipril absorption low-salt milk, salt substitutes: Possibly hyperkalemia
alcohol use: Possibly hypotension

Side Efect

CNS: Anxiety, chills, confusion, dizziness, drowsiness, fatigue, fever, headache, malaise, mood changes, nervousness, sleep disturbance, stroke, syncope
CV: Angina, arrhythmias, chest pain, hypotension, MI, orthostatic hypotension, palpitations, peripheral edema
EENT: Dry mouth, hoarseness, laryngeal edema, mouth or tongue swelling, pharyngitis, rhinitis, sinusitis, taste perversion, tinnitus
GI: Abdominal distention or pain, anorexia, constipation, diarrhea, dysphagia, elevated liver function test results, hepatitis, increased appetite, nausea, pancreatitis, vomiting
GU: Azotemia, elevated BUN and serum creatinine and uric acid levels, interstitial nephritis, oliguria, proteinuria, renal insufficiency, urinary frequency
HEME: Agranulocytosis, bone marrow depression, elevated erythrocyte sedimentation rate, hemolytic anemia, leukocytosis, leukopenia, neutropenia, thrombocytopenia
MS: Arthralgia, leg heaviness or weakness, myalgia, myositis
RESP: Bronchospasm, cough, dyspnea, upper respiratory tract infection
SKIN: Alopecia, diaphoresis, flushing, onycholysis, pallor, pemphigus, photosensitivity, pruritus, rash, Stevens-Johnson syndrome, urticaria
Other: Anaphylaxis, angioedema (of arms, face, larynx, legs, lips, mucous membranes, tongue), flulike symptoms, hyperkalemia, hyponatremia, positive ANA titer

Cautions

WARNING Contact prescriber if patient is or may be pregnant. Moexipril may cause fetal or neonatal harm or death if used during second or third trimester.

Be aware that patient who already takes a diuretic should be medically supervised for several hours after first moexipril dose.

Administer drug 1 hour before meals.

Monitor blood pressure, leukocyte count, and liver and renal function test results during moexipril therapy.

Be aware that black patients may be less responsive to antihypertensive effect if moexipril is used alone to control blood pressure.

PATIENT SAFTY

Urge female patient to notify prescriber immediately if she is or may be pregnant.

Instruct patient to take moexipril at the same time each day, 1 hour before meals.

Direct patient to take a missed dose as soon as he remembers unless it’s nearly time for the next dose. Caution against doubling the dose.
WARNING Instruct patient to stop drug and seek immediate medical attention for hoarseness; swelling of tongue, glottis, larynx, face, hands, or feet; or sudden difficulty swallowing or breathing.

Caution patient not to stop drug without consulting prescriber, even if he feels better.

Inform patient about possible dizziness, especially after first dose and if he takes a diuretic.

Advise patient to change position slowly to minimize orthostatic hypotension.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to notify prescriber if he faints or experiences persistent dizziness.

Instruct patient to report evidence of infection (such as chills, fever, and sore throat), diarrhea, nausea, or vomiting, which may lead to dehydration-induced hypotension.

Advise patient to avoid alcohol during moexipril therapy because it may cause hypotension.

Instruct patient to check with prescriber before taking OTC .

Urge patient to avoid potassium supplements and potassium-containing salt substitutes unless prescriber allows them.

Advise patient to visit prescriber regularly to monitor progress.

Discuss importance of weight control and low-salt diet in managing hypertension.

Category

Chemical class: Dihydroindolone derivative
Therapeutic class: Antipsychotic drug

Pregnancy category: Not rated

Indications

To manage symptoms of psychotic disorders

ORALL

Adults and children age 12 and over. Initial: 50 to 75 mg daily in divided doses t.i.d. or q.i.d. Dosage increased to 100 mg daily in 3 to 4 days as needed. Maintenance: For mild psychosis, 5 to 15 mg t.i.d. or q.i.d.; for moderate psychosis, 10 to 25 mg t.i.d. or q.i.d.; for severe psychosis, 225 mg daily in divided doses. Maximum: 225 mg daily.
DOSAGE ADJUSTMENT Initial dosage reduced for elderly or debilitated patients. Route Onset Peak Duration P.O. Unknown Unknown 24–36 hr

Mechanism of Action

Occupies dopamine receptor sites in the reticular activating and limbic systems in the CNS. By blocking dopamine activity in these areas, molindone reduces the symptoms of psychosis, helping the patient to think and behave more coherently.

Contraindications

Hypersensitivity to molindone, its components, or other antipsychotic , including haloperidol, loxapine, phenothiazines, and thioxanthenes

Interactions

amphetamines: Decreased amphetamine effectiveness, decreased antipsychotic effecmolindone hydrochloride 693 M tiveness of molindone anesthetics, barbiturates, benzodiazepines, CNS depressants, opioid analgesics: Possibly prolonged and intensified CNS depressant effects antacids, antidiarrheals: Decreased molindone absorption anticholinergics, antidyskinetics, antihistamines: Possibly increased anticholinergic effects
beta blockers: Possibly increased effect of beta blocker bromocriptine: Possibly decreased therapeutic effects of bromocriptine and increased serum prolactin level extrapyramidal reaction–causing , such as amoxapine, haloperidol, loxapine, metoclopramide, olanzapine, phenothiazines, pimozide, rauwolfia alkaloids, risperidone, tacrine, and
thioxanthenes: Increased severity of extrapyramidal effects insulin, oral antidiabetic : Possibly increased serum glucose level levodopa: Inhibited antidyskinetic effects of levodopa, possibly decreased antipsychotic effects of molindone lithium: Increased risk of neurotoxicity, increased extrapyramidal effects MAO inhibitors, maprotiline, trazodone, tricyclic antidepressants: Possibly prolonged and intensified sedative or anticholinergic effects of all phenytoin, tetracycline: Interference with absorption of phenytoin and tetracycline
alcohol use: Prolonged and intensified CNS depression

Side Efect

CNS: Depression, drowsiness, euphoria, extrapyramidal reactions (such as akathisia, dystonia, motor restlessness, pseudoparkinsonism, and tardive dyskinesia), headache, hyperactivity, lack of coordination, neuroleptic malignant syndrome, tiredness
CV: Orthostatic hypotension, tachycardia, unstable blood pressure
EENT: Blinking or eyelid spasm, blurred vision, dry mouth, inability to move eyes, nasal congestion
ENDO: Breast engorgement, lactation
GI: Constipation, nausea
GU: Decreased libido, menstrual irregularities, urine retention
HEME: Agranulocytosis, leukopenia, neutropenia
MS: Muscle spasms of back, face, and neck; muscle twitching; twisting movements of the body; weakness or stiffness of limbs
RESP: Dyspnea
SKIN: Diaphoresis, pallor, rash
Other: Heatstroke

Cautions

Molindone shouldn’t be used to treat dementia-related psychosis in the elderly because of an increased mortality risk.
WARNING Assess patient for signs and symptoms of neuroleptic malignant syndrome, such as diaphoresis, dyspnea, fatigue, fever, incontinence, pallor, severe muscle stiffness, tachycardia, and unstable blood pressure; notify prescriber immediately if they occur. Expect to discontinue drug and begin intensive medical treatment. Monitor patient carefully for recurrence if antipsychotic therapy resumes.

Molindone shouldn’t be given to patients who have severe CNS depression or who are comatose because of drug’s CNS depressant effects.

Monitor elderly patients for orthostatic hypotension and symptoms of tardive dyskinesia, including blinking or eyelid spasms, involuntary movements of the limbs, and unusual facial expressions, because these patients may be sensitive to drug’s anticholinergic and extrapyramidal effects. Expect to reduce dosage or discontinue drug.

Give oral solution undiluted or mixed with water, carbonated beverage, fruit juice, or milk.

Monitor CBC often during first few months of therapy, especially if patient has low WBC count or history of druginduced leukopenia or neutropenia. If WBC count drops, and especially if neutrophil count drops below 1000/mm3, expect molindone to be discontinued. If neutropenia is significant, also monitor patient for fever or other evidence of infection and provide appropriate treatment, as prescribed.

PATIENT SAFTY

Instruct patient to follow treatment regimen and to notify prescriber before discontinuing drug because gradual dosage reduction may be needed.

Instruct patient not to take drug within 2 hours of taking an antacid. Advise him to take drug with food or a full glass of milk or water to reduce gastric irritation.

Instruct patient to take oral solution undiluted or mixed with water, carbonated beverage, fruit juice, or milk.

Urge patient to avoid alcohol consumption because of possible additive effects and hypotension.

Advise patient, especially an elderly patient, to rise slowly from a supine or seated position to avoid feeling dizzy, light-headed, or faint.

Explain that drug may reduce body’s response to heat. Tell patient to avoid temperature extremes, such as hot showers, tubs, or saunas. Urge caution during exercise.

Caution patient not to take OTC for colds or allergies during therapy because they can increase the risk of heatstroke and increase anticholinergic effects, such as blurred vision, constipation, dry mouth, and urine retention.

Inform patient and family members that maximum clinical improvement in symptoms may take several weeks or months.

Category

Chemical class: Glucocorticoid
Therapeutic class: Antiasthmatic, antiinflammatory

Pregnancy category: C

Indications

To manage symptoms of seasonal or perennial allergic rhinitis
NASAL SPRAY Adults and children 12 years and over. 100 mcg (2 sprays) in each nostril daily. Children ages 2 to 12. 50 mcg (1 spray) in each nostril daily. To maintain asthma control ORAL INHALATION Adults and children age 12 and over who have been taking bronchodilators alone or inhaled corticosteroids. Initial: 220 mcg (1 inhalation) once daily in evening. Maximum: 440 mcg (2 inhalations) daily given as 220 mcg (1 inhalation) b.i.d. or 440 mcg (1 inhalation) once daily. Adults and children age 12 and over who have taken oral corticosteroids. 440 mcg (2 inhalations) b.i.d. Children ages 4 to 11. 110 mcg (1 inhalation) once daily in evening.

Mechanism of Action

Inhibits the activity of cells and mediators active in the inflammatory response, possibly by decreasing influx of inflammatory cells into nasal passages and thereby decreasing nasal inflammation.

Contraindications

Hypersensitivity to mometasone or its components; recent septal ulcers, nasal surgery, or nasal trauma; status asthmaticus or other asthma episodes that require emergency care

Side Efect

CNS: Headache
CV: Chest pain
EENT: Cataracts, conjunctivitis, dry mouth, earache, epistaxis, glaucoma, nasal irritation, oral and pharyngeal candidiasis, otitis media, pharyngitis, rhinitis, sinusitis, throat tightness, unpleasant taste
ENDO: Adrenal insufficiency, growth suppression
GI: Diarrhea, dyspepsia, nausea, vomiting
GU: Dysmenorrhea
MS: Arthralgia, decreased bone mineral density, myalgia, pain
RESP: Asthma, bronchitis, bronchospasm, increased cough, upper respiratory tract infection, wheezing
SKIN: Urticaria
Other: Angioedema, flulike symptoms, viral infection

Cautions

Use mometasone cautiously if patient has tubercular infection; untreated fungal, bacterial, or systemic viral infection; or ocular herpes simplex.

If patient takes an oral corticosteroid, expect to taper it slowly 1 week after changing to mometasone. If patient takes prednisone, expect to reduce it by no more than 2.5 mg daily at weekly intervals, beginning at least 1 week after mometasone therapy starts. Monitor patient for symptoms of systemically active corticosteroid withdrawal such as joint and muscle pain, lassitude, and depression despite maintenance or even improvement of respiratory symptoms.
WARNING Assess patient switched from systemic corticosteroid to mometasone for adrenal insufficiency (fatigue, hypotension, lassitude, nausea, vomiting, weakness) during initial treatment and during stress, trauma, surgery, infection or an electrolyte-depleting condition. Notify prescriber immediately if signs or symptoms arise because adrenal insufficiency may be life-threatening. Hypothalamicpituitary-adrenal axis function may take several months to recover after systemic corticosteroids are discontinued. Abrupt withdrawal of mometasone also may precipitate adrenal insufficiency.

Notify prescriber immediately if patient has bronchospasm after mometasone oral inhalation, and expect to give a fast-acting inhaled bronchodilator, discontinue mometasone, and use an alternate drug.

Closely monitor a child’s growth pattern; drug may stunt growth.

Report oropharyngeal candidiasis, and expect patient to receive appropriate antifungal therapy while remaining on mometasone therapy. If candidiasis is severe, however, mometasone therapy may need to be temporarily halted.

PATIENT SAFTY

For
NASAL SPRAY, instruct patient to shake container before each use. Instruct her to blow her nose, tilt her head slightly forward, and insert tube into a nostril, pointing toward inner corner of eye, away from nasal septum. Tell her to hold the other nostril closed and spray while inhaling gently. Then have her repeat the procedure in the other nostril.

For oral inhalation, give patient these instructions for using inhaler: Remove cap only after placing inhaler in an upright position. Twist cap in counterclockwise while holding colored base, making sure indented arrow (on white portion of the inhaler directly above the colored base) is pointing to the dose counter. Removing the cap loads inhaler with drug, and the dose counter on the base will count down by one. Take a full breath in and out, and then place mouthpiece in your mouth. Firmly close your lips around mouthpiece, taking care not to cover ventilation holes on the inhaler. Then take a fast, deep breath.You may not taste, smell, or feel anything with the inhalation. After taking the breath, remove inhaler from your mouth and hold your breath for about 10 seconds. Don’t exhale into the inhaler. Wipe the mouthpiece dry, if needed, and replace the cap right away, turning it clockwise as you press down.You should hear a click when the cap is fully closed. Write down the date inhaler is opened, and discard it 45 days from that date or when dose counter reads 00, whichever comes first.

Instruct patient to gargle or rinse after each use of oral inhaler to help prevent mouth and throat dryness, relieve throat irritation, and prevent oropharyngeal infection.
WARNING Caution patient not to use mometasone oral inhalation to relieve acute bronchospasm and to notify prescriber if rescue inhaler is required more often or doesn’t seem to be as effective.

If patient switches from an oral corticosteroid to mometasone, advise her to carry or wear medical identification indicating the need for supplemental systemic corticosteroids during stress or severe asthma attack. Tell her to seek emergency care if either occurs.

Instruct patient to contact prescriber if symptoms persist or worsen after 3 weeks.

Caution patient to avoid exposure to chickenpox and measles and, if exposed, to contact prescriber immediately.

Category

Chemical class: Leukotriene receptor antagonist
Therapeutic class: Antiasthmatic

Pregnancy category: B

Indications

To prevent or treat asthma ORAL GRANULES Children ages 12 to 23 mo.4 mg daily in the evening. Maximum: 4 mg daily. CHEWABLE Children ages 6 to 14. 5 mg daily in the evening. Maximum: 5 mg daily. Children ages 2 to 5. 4 mg daily in the evening. Maximum: 4 mg daily. Adults and adolescents age 15 and over. 10 mg daily in the evening. Maximum: 10 mg daily. To treat seasonal allergic rhinitis ORAL GRANULES Children ages 2 to 5. 4 mg daily. CHEWABLE Children ages 6 to 14. 5 mg daily. Children ages 2 to 5. 4 mg daily. Adults and adolescents age 15 and over. 10 mg daily. To treat perennial allergic rhinitis ORAL GRANULES Children ages 6 months to 5 years. 4 mg daily. CHEWABLE Children ages 6 to 14. 5 mg daily. Children ages 2 to 5. 4 mg daily. Adults and adolescents age 15 and over. 10 mg daily. To prevent exercise-induced bronchoconstriction Adults and adolescents age 15 and over. 10 mg at least 2 hr before exercise. Maximum: 10 mg in 24 hr. Route Onset Peak Duration P.O. Unknown Unknown 24 hr

Mechanism of Action

Antagonizes receptors for cysteinyl leukotrienes, produced by arachidonic acid metabolism and released from mast cells, eosinophils, and other cells.When cysteinyl leukotrienes bind to receptors in bronchial airways, they increase endothelial membrane permeability, which leads to airway edema, smooth-muscle contraction, and altered activity of cells in asthma’s inflammatory process. Montelukast blocks these effects.

Interactions

phenobarbital: Decreased amount of circulating montelukast

Side Efect

CNS: Aggression, agitation, anxiousness, asthenia, depression, dizziness, dream abnormalities, fatigue, fever, hallucinations, headache, hostility, hypoesthesia, insomnia, irritability, paresthesia, restlessness, sleep walking, suicidal ideation, tremor
CV: Palpitations
EENT: Dental pain, epistaxis, laryngitis, nasal congestion, otitis media, pharyngitis, sinusitis
GI: Abdominal pain, cholestatic hepatitis, dyspepsia, elevated liver function test results, hepatotoxicity, indigestion, infectious gastroenteritis (in all patients); diarrhea, nausea (in children)
GU: Pyuria
RESP: Cough, upper respiratory tract infection
SKIN: Erythema nodosum, pruritus, rash, urticaria
Other: Anaphylaxis, angioedema (in all patients); flulike syndrome, viral infection (in children)

Cautions

WARNING Montelukast isn’t for acute asthma attack or status asthmaticus.

Montelukast shouldn’t be abruptly substituted for inhaled or oral corticosteroids; expect to taper corticosteroid dosage gradually, as directed.

Monitor patient for

Side Efect

, such as cardiac and pulmonary symptoms, eosinophilia, and vasculitis, in patient undergoing corticosteroid withdrawal. Notify prescriber if such reactions occur.

Watch patient closely for suicidal tendencies during montelukast therapy, especially when therapy starts or dosage changes.

Monitor patient for adverse neuropsychiatric effects and notify prescriber if present. Drug may need to be discontinued.

PATIENT SAFTY

Advise patient to take montelukast daily as prescribed, even when he feels well. Urge him not to decrease dosage or stop taking other prescribed asthma unless instructed by prescriber.

Caution patient not to use drug for acute asthma attack or status asthmaticus; make sure he has appropriate short-acting rescue drug available.

Tell parents administering oral granules to pour contents directly into the child’s mouth or mix with ice cream or cold or room temperature applesauce, carrots, or rice—but not liquids or other —just before administration. Liquids may be given after drug has been administered. Once packet is opened, the full dose must be administered within 15 minutes. Drug must not be stored for future use if mixed with food.

Instruct patient to notify prescriber if he needs a short-acting inhaled bronchodilator more often than usual, or more often than prescribed, to control symptoms.

Teach patient to use a peak flowmeter to determine his personal best expiratory volume.

Caution patient with aspirin sensitivity to avoid aspirin and NSAIDs during montelukast therapy. Montelukast may not effectively reduce bronchospasm in such a patient.

Inform patient (or parents of child) with phenylketonuria that chewable tablet contains phenylalanine.

Instruct patient to notify prescriber if she is or could be pregnant.

Urge family or caregiver to watch patient closely for abnormal behaviors, including suicidal tendencies, during therapy, and urge them to notify prescriber if present.

Category

Chemical class: Phenanthrene derivative
Therapeutic class: Analgesic

Pregnancy category: C

Controlled substance schedule: II

Indications

To relieve acute or chronic moderate to severe pain; as adjunct to treat pulmonary edema caused by left-sided heart failure; to supplement general, local, or regional anesthesia ,, SYRUP,
Adults. Initial: 10 to 30 mg every 4 hr, p.r.n. Children.Individualized dosage based on patient’s age, size, and need.
IV:
Adults. Initial: 15 mg (or more) followed by 0.8 to 10 mg/hr, increased as needed for effectiveness. Maintenance: 0.8 to 80 mg/hr. Children.0.01 to 0.04 mg/kg/hr postoperatively, 0.025 to 2.6 mg/kg/hr for severe chronic cancer pain, or 0.03 to 0.15 mg/kg/ hr for sickle cell crisis. Neonates.Initial: 0.010 mg/kg/hr (10 mcg/ kg/hr) postoperatively. Maintenance: 0.015 to 0.02 mg/kg/hr (15 to 20 mcg/kg/hr).
I.V.INJECTION
Adults. 2.5 to 15 mg injected slowly. Children.0.5 to 0.1 mg/kg given slowly. I.M. OR SUBCUTANEOUS INJECTION
Adults.Initial: 10 mg (based on 70-kg [154-lb] adult) every 4 hr. Maintenance: 5 to 20 mg. Children. Initial: 0.1 to 0.2 mg/kg every 4 hr. Maximum: 15 mg/dose. EPIDURAL INFUSION(PRESERVATIVE-FREE)
Adults. Initial: 2 to 4 mg/24 hr, increased by 1 to 2 mg/24 hr, as directed. EPIDURAL INJECTION(PRESERVATIVE-FREE)
Adults. Initial: 5 mg into lumbar region. If pain isn’t relieved after 1 hr, 1to 2-mg doses given at appropriate intervals to relieve pain. Maximum: 10 mg/24 hr.

INTRATHECAL

INJECTION(PRESERVATIVE-FREE)
Adults. 0.2 to 1 mg as a single dose. SUPPOSITORIES
Adults.10 to 30 mg every 4 hr, p.r.n. Children. Individualized dosage based on patient’s age, size, and need. To relieve chronic moderate to severe pain that requires opioids for more than a few days E.R
Adults. Individualized dosage given every 12 to 24 hr.
Adults. 30 mg every 12 hr. Dosage increased based on patient’s response. To relieve MI pain
I.V.INJECTION
Adults. 1 to 4 mg by slow I.V. injection. Repeated up to every 5 min, if needed. Maximum: 2 to 15 mg. To provide preoperative analgesia I.M. OR SUBCUTANEOUS INJECTION
Adults.5 to 20 mg given 45 to 60 min before surgery. Children. 0.05 to 0.1 mg/kg given 45 to 60 min before surgery. Maximum: 10 mg. To provide analgesia during labor I.M. OR SUBCUTANEOUS INJECTION
Adults. 10 mg, with subsequent doses based on patient’s response. Route Onset Peak Duration P.O. Unknown 1–2 hr 4–5 hr P.O.() Unknown Unknown 8–12 hr I.V. Unknown 20 min 4–5 hr I.M. 10–30 min 30–60 min 4–5 hr SubQ 10–30 min 50–90 min 4–5 hr Epidural 15–60 min Unknown Up to 24 hr Intrathecal 15–60 min Unknown Up to 24 hr P.R. 20–60 min Unknown Unknown

Mechanism of Action

Binds with and activates opioid receptors (mainly mu receptors) in brain and spinal cord to produce analgesia and euphoria.

Contraindications

For all drug for
MS: Asthma, hypersensitivity to morphine or its components, labor (premature delivery), prematurity (in infants), respiratory depression, upper airway obstruction For oral solution: Acute abdominal disorders, acute alcoholism, alcohol withdrawal syndrome, arrhythmias, brain tumor, head injuries, heart failure caused by chronic lung disease, increased intracranial or cerebrospinal pressure, recent biliary tract surgery, respiratory insufficiency, seizure disorders, severe CNS depression, surgical anastomosis, use within 14 days of an MAO inhibitor For I.V., I.M., or subcutaneous injection: Acute alcoholism, alcohol withdrawal syndrome, arrhythmias, brain tumor, heart failure caused by chronic lung disease, seizure disorders For epidural or intrathecal injection: Anticoagulant therapy, bleeding tendency, injection site infection, parenteral corticosteroid treatment (or other treatment or condition that prohibits drug delivery by intrathecal or epidural route) within 2 weeks

Interactions

amitriptyline, clomipramine, nortriptyline: Increased CNS and respiratory depression anticholinergics: Possibly severe constipation leading to ileus, urine retention antidiarrheals (such as loperamide and paregoric): CNS depression, possibly severe constipation antihistamines, chloral hydrate, glutethimide, MAO inhibitors, methocarbamol: Increased CNS and respiratory depressant effects antihypertensives, hypotension-producing : Increased hypotension, risk of orthostatic hypotension bupivacaine: Increased serum morphine level and possibly significant adverse effects buprenorphine: Decreased therapeutic effects of morphine, increased respiratory depression, possibly withdrawal symptoms
cimetidine: Increased analgesic and CNS and respiratory depressant effects CNS depressants (antiemetics, general anesthetics, hypnotics, phenothiazines, sedatives, tranquilizers): Possibly coma, hypotension, respiratory depression, severe sedation diuretics: Decreased diuretic efficacy hydroxyzine: Increased analgesic, CNS depressant, and hypotensive effects of morphine metoclopramide: Possibly antagonized metoclopramide effect on GI motility mixed agonist-antagonist analgesics: Possibly withdrawal symptoms naloxone: Antagonized analgesic and CNS and respiratory depressant effects of morphine, possibly withdrawal symptoms
naltrexone: Possibly induction or worsening of withdrawal symptoms if morphine given within 7 to 10 days before naltrexone neuromuscular blockers: Increased or prolonged respiratory depression opioid analgesics (such as alfentanil and sufentanil): Increased CNS and respiratory depression, increased hypotension zidovudine: Decreased zidovudine clearance
alcohol use: Increased CNS and respiratory depression, increased hypotension

Side Efect

CNS: Amnesia, anxiety, coma, confusion, decreased concentration, delirium, delusions, depression, dizziness, drowsiness, euphoria, fever, hallucinations, headache, insomnia, lethargy, light-headedness, malaise, psychosis, restlessness, sedation, seizures, syncope, tremor, unarousable, unresponsiveness
CV: Bradycardia, cardiac arrest, hypotension, orthostatic hypotension, palpitations, shock, tachycardia
EENT: Blurred vision, diplopia, dry mouth, laryngeal edema or laryngospasm (allergic), miosis, nystagmus, rhinitis
GI: Abdominal cramps or pain, anorexia, biliary tract spasm, constipation, diarrhea, dysphagia, elevated liver function test results, gastroesophageal reflux, hiccups, ileus and toxic megacolon (in patients with inflammatory bowel disease), intestinal obstruction, indigestion, nausea, vomiting
GU: Decreased ejaculate potency, decreased libido, difficult ejaculation, impotence, menstrual irregularities, oliguria, prolonged labor, urinary hesitancy, urine retention
HEME: Anemia, leukopenia, thrombocytopenia
MS: Arthralgia
RESP: Apnea, asthma exacerbation, atelectasis, bronchospasm, depressed cough reflex, hypoventilation, pulmonary edema, respiratory arrest and depression, wheezing
SKIN: Diaphoresis, flushing, pallor, pruritus, urticaria
Other: Allergic reaction; anaphylaxis; facial edema; injection site edema, pain, rash, or redness; physical and psychological dependence; withdrawal symptoms

Cautions

Use cautiously in patients about to undergo surgery of the biliary tract and patients with acute pancreatitis secondary to biliary tract disease because morphine may cause spasm of the sphincter of Oddi.

Store morphine at room temperature.

Before giving morphine, make sure opioid antagonist and equipment for oxygen delivery and respiration are available.

Before therapy, assess patient’s drug use, including all prescription and OTC .

Expect prescriber to start patient who has never received opioids on immediaterelease form and then switch to form if therapy must last longer than a few days.

Keep in mind that when morphine is given by epidural route, dosage must be individualized according to patient’s age, body mass, physical status, previous experience with opioids, risk factors for respiratory depression, and to be coadministered before or during surgery.

Give oral form with food or milk to minimize adverse GI reactions, if needed. Solution can be mixed with fruit juice to improve taste.

If needed, open capsules and sprinkle contents on applesauce (at room temperature or cooler) just before giving to patient. Make sure patient doesn’t chew or crush capsules or dissolve capsule’s pellets in his mouth.

Be aware that forms of morphine aren’t interchangeable.

Discard injection solution that is discolored or darker than pale yellow or that contains precipitates that don’t dissolve with shaking.
WARNING Don’t use highly concentrated solutions (such as 10 to 25 mg/ml) for single-dose I.V., I.M., or subcutaneous administration. These solutions are intended for use in continuous, controlled microinfusion devices.

For direct I.V. injection, dilute appropriate dose with 4 to 5 ml of sterile water for injection. Inject 2.5 to 15 mg directly into tubing of free-flowing I.V. solution over 4 to 5 minutes. Rapid I.V. injection may increase

Side Efect

.

For continuous I.V. infusion, dilute drug in D5W and administer with infusioncontrol device. Adjust dose and rate based on patient response, as prescribed.

Avoid I.M. route for long-term therapy because of injection site irritation.

During subcutaneous injection, take care to avoid injecting drug intradermally.

For intrathecal injection, expect prescriber to give no more than 2 ml of 0.5-mg/ml solution or 1 ml of 1-mg/ml solution. Expect intrathecal dosage to be about onetenth of epidural dosage.

If rectal suppository is too soft to insert, refrigerate for 30 minutes or run wrapped suppository under cold tap water.
WARNING Monitor respiratory and cardiomorphine sulfate 700 vascular status carefully and frequently during morphine therapy. Be alert for respiratory depression and hypotension.

Monitor patient with seizure disorder for increased seizure activity because morphine may worsen the disorder.

Monitor patient for excessive or persistent sedation; dosage may need to be adjusted.

If patient is receiving a continuous morphine infusion, watch for and notify prescriber about new neurologic signs or symptoms. Inflammatory masses (such as granulomas) have caused serious neurologic reactions, including paralysis.

Expect morphine to cause physical and psychological dependence; watch for drug tolerance and withdrawal, such as body aches, diaphoresis, diarrhea, fever, piloerection, rhinorrhea, sneezing, and yawning.

If tolerance to morphine develops, expect prescriber to increase dosage.

Morphine may have a prolonged duration and cumulative effect in patients with impaired hepatic or renal function. It also may prolong labor by reducing strength, duration, and frequency of uterine contractions.

When discontinuing morphine in patients receiving more than 30 mg daily, expect prescriber to reduce daily dose by about one-half for 2 days and then by 25% every 2 days thereafter until total dose reaches initial amount recommended for patients who haven’t received opioids (15 to 30 mg daily). This regimen minimizes the risk of withdrawal symptoms.

PATIENT SAFTY

Instruct patient to take morphine exactly as prescribed and not to change dosage without consulting prescriber.

Explain that patient may take tablets or capsules with food or milk to relieve GI distress and may mix oral solution with juice to improve taste.

Urge patient not to break, chew, or crush capsules and tablets to avoid rapid release and, possibly, toxicity.

For patient who has difficulty swallowing, suggest that he open capsules and sprinkle contents on food or liquids. Urge him to take drug immediately and not let capsule contents dissolve in his mouth.

Instruct patient to moisten rectal suppository before inserting it.

Urge patient to avoid alcohol and other CNS depressants during therapy.

Advise patient to avoid potentially hazardous activities during morphine therapy.

Tell patient to change positions slowly to minimize the orthostatic hypotension.

Instruct patient to notify prescriber about worsening or breakthrough pain.

Explain that morphine may be habitforming. Urge him to notify prescriber if he experiences anxiety, decreased appetite, excessive tearing, irritability, muscle aches or twitching, rapid heart rate, or yawning.

Advise female patient to notify prescriber if she becomes pregnant. Regular morphine use during pregnancy may cause physical dependence in fetus and withdrawal in neonate.

Category

Chemical class: Fluoroquinolone
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To treat acute sinusitis caused by Haemophilus influenzae, Moraxella catarrhalis, or Streptococcus pneumoniae; to treat mild to moderate community-acquired pneumonia caused by Chlamydia pneumoniae, H. influenzae, M. catarrhalis, Mycoplasma pneumoniae, or S. pneumoniae (including penicillinor multi-drug–resistant strains) ,
IV:
Adults.400 mg every 24 hr for 10 days. To treat acute exacerbation of chronic bronchitis caused by H. influenzae, H. parainfluenzae, Klebsiella pneumoniae, M. catarrhalis, S. pneumoniae, or Staphylococcus aureus ,
IV:
Adults.400 mg every 24 hr for 5 days. To treat uncomplicated skin and softtissue infections caused by S. aureus or Streptococcus pyogenes ,
IV:
Adults.400 mg every 24 hr for 7 days. moxifloxacin hydrochloride 701 M To treat complicated skin and skin structure infections caused by S. aureus, E. coli, K. pneumoniae, or Enterobacter cloacae ,
IV:
Adults. 400 mg every 24 hr for 7 to 21 days. To treat complicated intra-abdominal infections, including polymicrobial infections such as abscesses caused by E.coli, Bacteroides fragilis, Streptococcus anginosus, Streptococcus constellatus, Enterococcus faecalis, Proteus mirabilis, Clostridium perfringens, Bacteroides thetaiotaomicron, or Peptostreptococcus species ,
IV:
Adults. 400 mg every 24 hr for 5 to 14 days with initial dosage given as I.V. infusion.

Mechanism of Action

Inhibits synthesis of bacterial enzyme DNA gyrase by counteracting excessive supercoiling of DNA during replication or transcription. Inhibiting DNA gyrase causes rapidand slow-growing bacterial cells to die.

Incompatibilities

Don;t infuse I.V. moxifloxacin simultaneously through the same I.V. line with other I.V. substances, additives, or .

Contraindications

Hypersensitivity to moxifloxacin, other fluoroquinolones, or their components

Interactions

aluminumor magnesium-containing antacids; drug formulations with divalent or trivalent cations, such as didanosine chewable buffered tablets or powder for oral solution; metal cations, such as iron; multivitamins containing iron or zinc; sucralfate: Possibly substantial interference with moxifloxacin absorption, causing low blood moxifloxacin level class IA antiarrhythmics, such as quinidine; class III antiarrhythmics, such as sotalol; other known to prolong QTc interval, such as disopyramide and pentamidine: Possibly prolonged QTc interval corticosteroids: Increased risk of Achilles and other tendon ruptures
NSAIDs: Increased risk of CNS stimulation and seizures
warfarin: Possibly increased anticoagulation

Side Efect

CNS: Abnormal gait, altered coordination, dizziness, fever, headache, psychosis, psychotic reaction, seizures, syncope
CV: Hypertension, hypotension, palpitations, peripheral edema, prolonged QTc interval, tachycardia, vasculitis, vasodilation, ventricular tachyarrhythmias
EENT: Altered taste, laryngeal edema
GI: Abdominal pain, abnormal liver function test results, acute hepatic necrosis or failure, cholestatic hepatitis, diarrhea, dyspepsia, hepatitis, jaundice, nausea, pseudomembranous colitis, vomiting
GU: Acute renal insufficiency or failure, interstitial nephritis
HEME: Agranulocytosis, aplastic anemia, eosinophilia, hemolytic anemia, leukopenia, pancytopenia, prolonged PT, thrombocytopenia
MS: Arthralgia, myalgia, tendon inflammation, pain, or rupture
RESP: Allergic pneumonitis
SKIN: Photosensitivity, rash, StevensJohnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, anaphylactic shock, angioedema, serum sickness, worsening of myasthenia gravis

Cautions

Use cautiously in patients with liver dysfunction, including cirrhosis, because drug may adversely affect liver function.

Obtain a fluid or tissue specimen for culture and sensitivity, as ordered. Expect to begin therapy before results are available.
WARNING Before starting moxifloxacin therapy, determine if patient takes a class IA antiarrhythmic, such as quinidine; a class III antiarrhythmic, such as sotalol; or other that prolong the QTc interval, such as antipsychotics, cisapride, erythromycin, or tricyclic antidepressants. These should be avoided in patients taking moxifloxacin because they may prolong the QTc interval and lead to life-threatening ventricular tachycardia or torsades de pointes. Monitor patient closely throughout therapy, especially if he has significant bradycardia or acute myocardial ischemia because these conditions increase risk of prolonging the QTc interval.

Infuse drug over 60 minutes with readymoxifloxacin hydrochloride 702 to-use flexible bags with 400 mg of moxifloxacin in 250 ml of 0.8% saline. Don’t dilute further.

If giving through Y-type tubing or piggyback, stop other solutions during moxifloxacin infusion, and flush the line before and after infusion with a compatible solution, such as normal saline solution, 1M sodium chloride, 5% dextrose, sterile water for injection, 10% dextrose, or lactated Ringer’s. Also flush line before and after giving other in same I.V. line.

Don’t refrigerate I.V. moxifloxacin readyto-use bags because precipitation will occur. Discard any unused portion; premixed bags are for single-use only.

Expect to obtain a 12-lead ECG to assess patient for prolonged QTc interval. Ask patient if he or a blood relative has a history of prolonged QTc interval. Monitor elderly patients closely; they may have increased risk of prolonged QT interval.

If patient has hypokalemia, expect to correct it before beginning moxifloxacin therapy to prevent arrhythmias.

Determine if patient has a history of CNS disorder, such as cerebral arteriosclerosis or epilepsy, because drug may lower seizure threshold. Notify prescriber before starting drug, and take seizure precautions.

If profuse, watery diarrhea develops, contact prescriber and expect to obtain a stool specimen to rule out pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold moxifloxacin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Monitor serum potassium level, as ordered, during therapy to assess for hypokalemia.

Keep emergency resuscitation equipment readily available, and observe for evidence of hypersensitivity, such as angioedema, dyspnea, and urticaria. If you suspect anaphylaxis, prepare to give epinephrine, corticosteroids, and diphenhydramine, as prescribed.

Monitor patients who are prone to tendinitis, such as the elderly, athletes, and those taking corticosteroids, for complaints of tendon pain, inflammation, or rupture. If present, notify prescriber and expect to discontinue moxifloxacin, place patient on bedrest with no exercise of affected limb, and obtain diagnostic tests to confirm rupture.

PATIENT SAFTY

Urge patient to notify prescriber at once about palpitations or fainting because they may indicate a serious arrhythmia.

Teach patient to take drug at least 4 hours before and 8 hours after aluminumor magnesium-containing antacids, didanosine chewable buffered tablets or oral solution prepared from powder, multivitamins containing iron or zinc, or sucralfate.

Urge patient to drink plenty of fluids while taking moxifloxacin.

Caution patient to stop drug and notify prescriber if he has trouble breathing, a rash, or other signs of an allergic reaction.

Urge patient to stop any exercise and contact prescriber immediately if he develops tendon inflammation, pain, or rupture.

Caution patient to avoid hazardous activities until adverse CNS effects are known.

Urge patient to tell prescriber if diarrhea develops, even more than 2 months after moxifloxacin therapy ends.

Caution patient to complete the prescribed course of therapy even if he feels better before it’s completed.

Tell patient to avoid excessive exposure to sunlight or artificial ultraviolet light because severe sunburn may result. Instruct patient to notify prescriber if sunburn develops because moxifloxacin may need to be discontinued.

Category

Chemical class: 2-morpholinoethyl ester of mycophenolic acid
Therapeutic class: Immunosuppressant

Pregnancy category: D

Indications

To prevent organ rejection in patients receiving allogenic kidney transplants , ORAL SUSPENSION,,
IV:
Adults. 1 g (over 2 hr for I.V. infusion) b.i.d.
Adults.720 mg b.i.d. SUSPENSION Children with body surface area less than 1.25 m2. 600 mg/m2 b.i.d. Maximum: 2 g (10 ml) daily. Children with body surface area of 1.25 m2to 1.5 m2. 750 mg b.i.d. , Children with body surface area greater than 1.5 m2.1 g b.i.d. To prevent organ rejection in patients receiving allogenic heart transplants , ORAL SUSPENSION,,
IV:
Adults. 1.5 g (over 2 hr for I.V. infusion) b.i.d. To prevent organ rejection in patients receiving allogenic liver transplants
IV:
Adults.1 g infused over 2 hr b.i.d. , ORAL SUSPENSION,
Adults.1.5 g b.i.d.

Mechanism of Action

Hydrolyzes to form mycophenolic acid (MPA), which inhibits guanosine nucleotide synthesis and proliferation of T and B lymphocytes. MPA also suppresses antibody formation by B lymphocytes and prevents glycosylation of lymphocyte and monocyte glycoproteins involved in adhesion to endothelial cells. MPA also may inhibit leukocytes from sites of inflammation and graft rejection, which may explain how mycophenolate mofetil prolongs allogeneic transplant survival.

Incompatibilities

Don’t mix or give mycophenolate mofetil hydrochloride in same infusion catheter with other I.V. or admixtures.

Contraindications

Hypersensitivity to mycophenolate mofetil, mycophenolic acid, or any of its components; hypersensitivity to polysorbate 80 (I.V. form)

Interactions

acyclovir, ganciclovir, probenecid: Increased plasma levels of both amoxicillin plus clavulanic acid, cholestyramine, cyclosporine, metronidazole, norfloxacin,
rifampin: Decreased plasma level of mycophenolate mofetil antacids with magnesium and aluminum hydroxides, sevelamer: Decreased absorption of oral mycophenolate mofetil azathioprine: Increased bone marrow suppression live vaccines: Decreased effectiveness of live vaccines oral contraceptives: Possibly decreased effectiveness of oral contraceptives

Side Efect

CNS: Agitation, anxiety, chills, confusion, delirium, depression, dizziness, emotional lability, fever, hallucinations, headache, hypertonia, hypesthesia, insomnia, malaise, meningitis, nervousness, neuropathy, paresthesia, progressive multifocal leukoencephalopathy, psychosis, seizure, somnolence, syncope, thinking abnormality, tremor, vertigo
CV: Angina pectoris, arrhythmias, arterial thrombosis, atrial fibrillation or flutter, bradycardia, cardiac arrest, CV disorder, congestive heart failure, extrasystole, generalized edema, hemorrhage, hypercholesterolemia, hyperlipemia, hypertension, hypotension, increased lactic dehydrogenase, increased SGOT and SGPT, increased venous pressure, infectious endocarditis, orthostatic hypotension, palpitations, pericardial effusion, peripheral edema, peripheral vascular disorder, pulmonary edema or hypertension, supraventricular tachycardia, thrombosis, vasodilation, vasospasm, ventricular extrasystole, ventricular tachycardia
EENT: Amblyopia, cataract, conjunctivitis, deafness, dry mouth, ear disorder or pain, epistaxis, eye hemorrhage, gingivitis, gum hyperplasia, lacrimation disorder, mouth ulceration, oral candidiasis, pharyngitis, rhinitis, sinusitis, stomatitis, tinnitus, vision abnormality, voice alteration
ENDO: Cushing’s syndrome, diabetes mellitus, hypercalcemia, hypocalcemia, hypoglycemia, hypothyroidism, parathyroid disorder
GI: Abdomen enlargement or pain, anorexia, ascites, cholangitis, cholestatic jaundice, colitis, constipation, diarrhea, dyspepsia, dysphagia, esophagitis, flatulence, gastritis, gastroenteritis, GI hemorrhage, GI infection, GI candidiasis, hepatitis, hernia, ileus, jaundice, liver damage, liver function test abnormalities, melena, nausea, pancreatitis, peritonitis, rectal disorder, stomach ulcer, vomiting
GU: Albuminuria; bilirubinemia; BK virus– related nephropathy; dysuria; hematuria; hydronephrosis; impotence; increased BUN or creatinine levels; kidney tubular necrosis; nocturia; oliguria; pain; prostatic disorder; pyelonephritis; renal failure; scrotal edema, urinary tract disorder or infection; urine abnormality, frequency, incontinence, or retention
HEME: Anemia, coagulation disorder, hypochromic anemia, increased prothrombin time or thromboplastin time, leukocytosis, leukopenia, polyhemia, pure red cell aplasia, thrombocytopenia
MS: Arthralgia; back, neck or pelvic pain; joint disorder; leg cramps; myalgia; myasthenia; osteoporosis
RESP: Apnea; asthma; atelectasis; bronchitis; cough; dyspnea; hemoptysis; hyperventilation; hypoxia; lung edema; pleural effusion; pneumonia; pneumothorax; pulmonary fibrosis; respiratory acidosis, candidiasis, neoplasm, or pain; sputum increase
SKIN: Abscess; acne; cellulite; ecchymosis; fungal dermatitis; pallor; petechia; pruritus; rash; benign neoplasm, carcinoma, hypertrophy, or ulcer; sweating; vesiculobullous rash
Other: Abnormal healing, accidental injury, acidosis, activation of latent infections (such as tuberculosis), alkalosis, alopecia, cyst, dehydration, facial edema, flulike syndrome, gout, hiccup, hirsutism, hyperkalemia, hyperuricemia, hypervolemia, hypochloremia, hypokalemia, hypomagnesemia, hyponatremia, hypoproteinemia, hypophosphatemia, increased alkaline phosphatase, increased gamma glutamyl transpeptidase, infection, lymphoma, malignancies, sepsis, thirst, weight gain or loss

Cautions

Before starting mycophentolate therapy in a woman of childbearing potential, make sure she has a negative pregnancy test within 1 week of starting therapy, using a test with a sensitivity of at least 25 mIU/ ml. Therapy shouldn’t start until results are confirmed.

Expect to give I.V. form within 24 hours of transplantation and for no longer than 14 days. Expect to switch patient to oral form as soon as possible, as ordered.

Expect to administer oral form of drug as soon as possible following transplantation.

When preparing oral suspension or I.V. form, avoid inhalation or direct contact with skin or mucous membranes. If contact occurs, wash area thoroughly with soap and water and rinse eyes with water.

To prepare oral suspension, tap closed bottle several times to loosen powder and then measure 94 ml of water in a graduated cylinder. Add half of the water to the bottle and shake for about 1 minute. Then add reminder of water and shake again for 1 minute. Remove child-resistant cap and push bottle adapter into neck of bottle. Close bottle tightly with child-resistant cap. Be aware that the suspension bottle may become cold immediately after reconstitution.

Know that oral suspension can be administered by 8F or larger nasogastric tube.

When giving oral suspension, don’t mix with any other . Ask patient about history of phenylketonuria before initial administration because oral suspension contains aspartame.

Don’t open or crush capsules. If necessary, use the oral suspension.

Handle I.V. form similarly to a chemotherapeutic drug because mycophenolate mofetil is genotoxic and embryotoxic and may have mutagenic properties.

Know that I.V. form must be reconstituted and diluted to 6 mg/ml using 5% dextrose injection USP. Inject 14 ml 5% dextrose injection USP into each vial (2 vials will be needed for each 1-g dose; 3 vials for each 1.5-g dose), then shake gently. Further dilute a 1-g dose by adding 2 reconstituted vials to 140 ml of 5% dextrose injection USP; dilute a 1.5-g dose by adding 3 reconstituted vials to 210 ml of 5% dextrose injection USP.

Be aware that I.V. form should be administered within 4 hours of constitution as an infusion and over no less than 2 hours. Never administer by rapid or bolus I.V. injection.

Know that cyclosporine and corticosteroids should be used with mycophenolate mofetil therapy.

Obtain CBC weekly during first month of therapy, twice monthly for the second and third months of therapy, and then monthly through the first year, as ordered.

Monitor patient closely for adverse reactions because drug has many adverse effects, some of which can be serious or severe.

Expect to stop drug or reduce the dose and provide supportive care, as ordered, if neutropenia develops.
WARNING Mycophenolate mofetil therapy has been associated with progressive multifocal leukoencephalopathy that can be life-threatening. Monitor patient for hemiparesis, apathy, confusion, cognitive deficiencies, and ataxia. Report suspicions of disorder immediately to prescriber.

PATIENT SAFTY

Advise women of childbearing age that two forms of contraceptives should be used simultaneously before beginning mycophenolate mofetil therapy and for 6 weeks following discontinuation of therapy because of potential for fetal harm. Inform women who use oral contraceptives that drug may decrease effectiveness of oral contraceptives. Urge patient to notify prescriber immediately if pregnancy occurs.

Before therapy starts, tell patient about increased risk of lymphomas or other malignancies. Tell patient to report any unusual signs or symptoms to prescriber.

Tell patient to take oral form of drug on an empty stomach.

Inform patient prescribed oral suspension that it contains aspartame, which is a source of phenylalanine.

Instruct patient not to crush tablets or capsules or open capsules.

Inform patient not to receive live vaccines during therapy. Urge him to avoid people who have received such vaccines or to wear a protective mask when he’s around them.

Tell patient to report any serious or ongoing

Side Efect

, especially neurologic abnormalities, to prescriber immediately.

Caution patient to avoid contact with people who have infections because drug causes immunosuppression.

Urge patient to report any signs of infection, unexpected bruising or bleeding, or any other sign of bone marrow depression immediately.

Tell patient that frequent laboratory tests may be needed during therapy. Stress that having these tests done is essential to continuing therapy.

Advise patient to avoid exposure to direct sunlight and UV light and to wear sunscreen when outdoors because of increased risk for skin cancer.

Advise patient not to take antacids at the same time as oral mycophenolate mofetil because some antacids can decrease drug’s absorption.

Tell patient to report unusual tiredness, lack of energy, paleness, dizziness, or fainting because dosage may need to be reduced or drug discontinued.

Stress importance of follow-up care to monitor the drug’s effectiveness and possible adverse effects because of the increased risk for cancer and infections as a result of immunosuppression. Inform patient of the need for periodic laboratory tests.

Category

Chemical class: Naphthylalkanone derivative
Therapeutic class: Anti-inflammatory, antirheumatic

Pregnancy category: C

(first trimester), Not rated (later trimesters)

Indications

To relieve symptoms of acute and chronic osteoarthritis and rheumatoid arthritis
Adults. Initial: 1 g daily as a single dose or in divided doses b.i.d., increased to 1.5 to 2 g daily in divided doses b.i.d. Maintenance: Adjusted according to clinical response. Maximum: 2 g daily.

Mechanism of Action

Blocks activity of cyclooxygenase, the enzyme needed to synthesize prostaglandins, which mediate the inflammatory response and cause local vasodilation, swelling, and pain. Prostaglandins also promote pain transmission from periphery to spinal cord. By blocking cyclooxygenase and inhibiting prostaglandins, the NSAID nabumetone reduces inflammatory symptoms and relieves pain.

Contraindications

Angioedema, asthma, bronchospasm, nasal polyps, rhinitis, or urticaria induced by aspirin, iodides, or other NSAIDs

Interactions

acetaminophen (long-term use): Increased risk of adverse renal effects anticoagulants, thrombolytics: Increased risk of GI bleeding antihypertensives: Decreased antihypertensive effectiveness
beta blockers: Decreased antihypertensive effects of beta blockers bone marrow depressants, such as aldesleukin and cisplatin: Increased risk of leukopenia and thrombocytopenia cefamandole, cefoperazone, cefotetan, plicamycin,
valproic acid: Increased risk of hypoprothrombinemia and bleeding colchicine, other NSAIDs, salicylates: Increased GI irritability and bleeding cyclosporine, gold compounds, nephrotoxic : Increased risk of nephrotoxicity digoxin: Increased blood digoxin level and risk of digitalis toxicity diuretics: Decreased diuretic effectiveness glucocorticoids, potassium supplements: Increased GI irritability and bleeding insulin, oral antidiabetic : Increased effects of these ; risk of hypoglycemia lithium: Increased risk of lithium toxicity methotrexate: Increased risk of methotrexate toxicity probenecid: Increased risk of nabumetone toxicity
alcohol use: Increased GI irritability and bleeding

Side Efect

CNS: Drowsiness, fatigue, fever, headache, nervousness, seizures, stroke, vertigo
CV: Edema, hypertension, MI, tachycardia
EENT: Dry mouth, pharyngitis, stomatitis, tinnitus
GI: Abdominal pain, anorexia, constipation, diarrhea, diverticulitis, dyspepsia, dysphagia, esophagitis, flatulence, gastritis, gastroenteritis, gastroesophageal reflux disease, GI bleeding and ulceration, hepatic dysfunction, indigestion, jaundice, melena, nausea, perforation of stomach or intestines, stomatitis, vomiting
GU: Albuminuria, azotemia, interstitial nephritis, nephrotic syndrome
HEME: Agranulocytosis, anemia, eosinophilia, granulocytopenia, hemolytic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia
MS: Muscle spasms, myalgia
RESP: Asthma, pneumonitis, respiratory depression
SKIN: Alopecia, erythema multiforme, photosensitivity, pruritus, rash, StevensJohnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, angioedema

Cautions

Use nabumetone with extreme caution in patients with a history of ulcer disease or GI bleeding because NSAIDs such as nabumetone increase risk of GI bleeding and ulceration. Expect to use nabumetone for shortest time possible in these patients.

Be aware that serious GI tract ulceration, bleeding, and perforation may occur without
WARNING symptoms. Elderly patients are at greater risk. To minimize risk, give drug with food. If GI distress occurs, withhold drug and notify prescriber immediately.

Use nabumetone cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.
WARNING Monitor patient closely for thrombotic events, including MI and stroke, because NSAIDs increase the risk.

Monitor patient—especially if elderly or receiving long-term nabumetone therapy—for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results because, rarely, elevations may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in elderly patients, patients taking diuretics or ACE inhibitors, and patients with heart failure, impaired renal function, or hepatic dysfunction; nabumetone may cause renal failure.

Monitor CBC for decreased hemoglobin and hematocrit; drug may worsen anemia.
WARNING If patient has bone marrow suppression or is receiving treatment with an antineoplastic, monitor laboratory results (including WBC count), and watch for evidence of infection because antiinflammatory and antipyretic actions of nabumetone may mask signs and symptoms, such as fever and pain.

Assess patient’s skin regularly for signs of rash or other hypersensitivity reaction because nabumetone is an NSAID and may cause serious skin reactions without
WARNING, even in patients with no history of NSAID sensivitity. At first sign of reaction, stop drug and notify prescriber.

Assess patient for severe hepatic reactions, including jaundice. Stop drug, as prescribed, if symptoms persist.

PATIENT SAFTY

Instruct patient to take nabumetone with food to reduce GI distress.

Advise patient to take drug with a full glass of water and to remain upright for 15 to 30 minutes afterward to prevent drug from lodging in esophagus and causing irritation.

Tell patient not to increase dose or frequency without consulting prescriber.

Urge patient to avoid alcohol to reduce risk of GI bleeding.

Inform patient that regular laboratory tests are needed to check for drug toxicity during long-term therapy.

Caution pregnant patient not to take NSAIDs such as nabumetone during the last trimester because they may cause premature closure of the ductus arteriosus.

Explain that nabumetone may increase the risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.

Explain that nabumetone may increase the risk of serious adverse GI reactions; stress the importance of seeking immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.

Alert patient to rare but serious skin reactions. Urge her to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity.

Category

Chemical class: Nonselective beta blocker
Therapeutic class: Antianginal, antihypertensive

Pregnancy category: C

Indications

To manage hypertension, alone or with other antihypertensives
Adults. Initial: 40 mg daily, increased by 40 to 80 mg daily every 7 days, as prescribed. Maintenance: 40 to 80 mg daily. Maximum: 320 mg daily. To manage angina pectoris as long-term therapy
Adults. Initial: 40 mg daily, increased by 40 to 80 mg daily every 3 to 7 days, as prescribed. Maintenance: 40 to 80 mg daily. Maximum: 240 mg daily.
DOSAGE ADJUSTMENT Interval possibly increased to every 24 to 36 hr if creatinine clearance is 31 to 50 ml/min/1.73 m2; to every 24 to 48 hr if it’s 10 to 30 ml/min/ 1.73 m2; or to every 40 to 60 hr if it’s less than 10 ml/min/1.73 m2. Route Onset Peak Duration P.O. Up to 5 days 4 hr 24 hr

Mechanism of Action

Selectively blocks alpha1and beta2receptors in vascular smooth muscle and beta1receptors in the heart, thereby reducing peripheral vascular resistance and blood pressure. Potent beta blockade decreases cardiac excitability, cardiac output, and myocardial oxygen demand, thus reducing angina. It also prevents reflex tachycardia, which typically occurs with most alpha blockers.

Contraindications

Asthma; bronchospasm; cardiogenic shock; heart failure; hypersensitivity to nadolol, other beta blockers, or their components; secondor third-degree AV block; severe COPD; sinus bradycardia

Interactions

allergen immunotherapy, allergenic extracts for skin testing: Increased risk of serious systemic reactions or anaphylaxis amiodarone: Increased risk of conduction abnormalities and negative inotropic effects beta blockers, digoxin: Increased risk of bradycardia calcium channel blockers: Increased risk of bradycardia
cimetidine: Possibly increased effects of nadolol clonidine, guanabenz: Impaired blood pressure control diazoxide, nitroglycerin: Increased risk of hypotension estrogens,
NSAIDs: Possibly reduced antihypertensive effect of nadolol general anesthetics: Increased risk of hypotension and myocardial depression insulin, oral antidiabetic : Possibly increased risk of hyperglycemia and impaired recovery from hypoglycemia, masking of signs of hypoglycemia lidocaine: Increased risk of lidocaine toxicity neuromuscular blockers: Possibly prolonged action of these phenothiazines: Possibly increased blood levels of both reserpine: Increased risk of bradycardia and hypotension sympathomimetics with alphaand betaadrenergic effects, such as pseudoephedrine: Possibly hypertension, excessive bradycardia, and heart block xanthines, such as theophyllines: Possibly decreased therapeutic effects of both

Side Efect

CNS: Anxiety, depression, dizziness, drowsiness, fatigue, headache, paresthesia, syncope, vertigo, weakness, yawning
CV: Bradycardia, chest pain, edema, heart block, heart failure, hypotension, orthostatic hypotension, ventricular arrhythmias
EENT: Nasal congestion, taste perversion
GI: Dyspepsia, elevated liver function test results, hepatic necrosis, hepatitis, nausea, vomiting
GU: Ejaculation failure, impotence
RESP: Cough, dyspnea, wheezing
SKIN: Jaundice, pruritus, scalp tingling Nursing Complications

Use nadolol cautiously in patients with diabetes mellitus because it may prolong or worsen hypoglycemia by interfering with glycogenolysis.

Anticipate that drug may worsen psoriasis and, in patients with myasthenia gravis, muscle weakness and diplopia.
WARNING Withdraw drug gradually over 2 weeks, or as ordered, to avoid MI caused by unopposed beta stimulation or thyroid storm caused by underlying hyperthyroidism. Expect drug to mask tachycardia caused by hyperthyroidism.

PATIENT SAFTY

Teach patient how to take her radial pulse, and direct her to do so before each dose of nadolol.

Instruct patient to notify prescriber if pulse rate falls below 60 beats/minute.

Caution patient not to stop taking nadolol abruptly or change dosage. Tell her to take a missed dose as soon as possible unless it’s within 8 hours of the next scheduled dose.

Advise patient with diabetes to check blood glucose level often because nadolol may mask signs of hypoglycemia, such as tachycardia.

Review signs of impending heart failure, and urge patient to notify prescriber immediately if they occur.

Category

Chemical class: Decapeptide, gonadotropinreleasing hormone analogue
Therapeutic class: Antiendometriotic, gonadal hormone inhibitor

Pregnancy category: X

Indications

To treat endometriosis NASAL INHALATION
Adults. 1 spray (200 mcg) into a nostril every morning and 1 spray into other nostril every evening for up to 6 mo. If amenorrhea doesn’t occur in 2 mo, dosage increased, as prescribed, to 800 mcg daily in divided doses. To treat gonadotropin-dependent precocious puberty NASAL INHALATION Children at puberty. 2 sprays (400 mcg) into each nostril every morning and evening. Maximum: 1,800 mcg daily in divided doses t.i.d.

Mechanism of Action

Stimulates release of the gonadotropins luteinizing hormone (LH) and folliclestimulating hormone (FSH), which temporarily increase ovarian steroidogenesis. Within 1 month, however, repeated administration of nafarelin halts pituitary gland stimulation and decreases LH and FSH secretion. This action decreases estrogen level, which improves symptoms of endometriosis. In children, repeated nafarelin administration returns LH and FSH to prepubescent levels, stopping development of secondary sex characteristics and slowing bone growth. Route Onset Peak Duration Nasal 60–120 20 days 3–6 mo days*

Contraindications

Breast-feeding; hypersensitivity to gonadotropin-releasing hormones, gonadotropinreleasing hormone analogues, nafarelin, or their components; pregnancy; undiagnosed vaginal bleeding

Interactions

nasal decongestants: Possibly impaired nafarelin absorption

Side Efect

CNS: Asthenia, depression, fever, headache, mood changes, paresthesia
CV: Chest pain, edema, hot flashes, palpitations
EENT: Eye pain, rhinitis
ENDO: Galactorrhea, gynecomastia, transient increase in pubic hair growth
GU: Hypermenorrhea, hypertrophy of female genitalia, impotence, libido changes, menstrual irregularities, ovarian cysts, uterine bleeding, vaginal dryness, vaginal spotting between menses
MS: Arthralgia, decreased bone density, myalgia
RESP: Dyspnea
SKIN: Acne, hirsutism, rash, seborrhea, skin discoloration (brown)
Other: Body odor

Cautions

Be aware that pregnancy must be ruled out before nafarelin therapy starts and that drug isn’t recommended for use by breastfeeding women.

Expect to start treatment for endometriosis between days 2 and 4 of menstrual cycle. Menses should cease after 6 weeks of treatment. Continued menses may indinafarelin acetate 710 * For gonadal hormone inhibitor effects, 4 wk. For antiendometriotic effects. cate lack of compliance.

Be aware that bone loss may increase if endometriosis treatment lasts longer than 6 months. Safety of retreatment after 6 months is unknown.

Avoid giving nasal decongestant within 2 hours after nafarelin because it may impair nafarelin absorption.

Be aware that prescriber will regularly monitor serum hormone levels in patient with gonadotropin-dependent precocious puberty, especially during first 6 to 8 weeks of therapy, to ensure rapid suppression of pituitary function.

PATIENT SAFTY

Instruct patient to comply with prescriber’s instructions for administering nafarelin to obtain desired drug effects.

Instruct patient to tilt her head back while administering nafarelin to enhance absorption; urge her to try not to sneeze afterward.

Caution patient not to change dosage without consulting prescriber.

Counsel patient to use nonhormonal contraception and to notify prescriber if she is or could be pregnant.

Direct patient not to use nasal decongestant within 2 hours after using nafarelin. If rhinitis occurs, urge her to contact prescriber for instructions.

Teach patient how to cope with adverse reactions to help maximize compliance.

Inform patient with endometriosis that drug should cause menses to stop. Urge her to notify prescriber if periods fail to stop even though she’s taking drug exactly as prescribed.

Advise patient with endometriosis to avoid alcohol and tobacco during therapy because they increase bone loss.

Inform patient with gonadotropin-dependent precocious puberty that signs of puberty will persist during first month of treatment. If they don’t resolve within 2 months, advise patient or parents to notify prescriber.

Tell patient with gonadotropin-dependent precocious puberty that prescriber will assess bone growth velocity and bone age during first 3 to 6 months of therapy.

Reassure parents of child with precocious puberty that child will resume growing when treatment stops.

Category

Chemical class: Penicillin
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat infections caused by penicillinase-producing Staphylococcus aureus , Adults and adolescents. 250 to 1,000 mg every 4 to 6 hr. Maximum: 6,000 mg daily. Children over age 1 month. 6.25 to 12.5 mg/kg every 6 hr. Neonates. 10 mg/kg every 6 to 8 hr.
IV: Adults and adolescents. 500 to 1,500 mg every 4 hr. Maximum: 20,000 mg daily. Children from birth to age 12.10 to 20 mg/ kg every 4 hr, or 20 to 40 mg/kg every 8 hr.
I.M.INJECTION Adults and adolescents. 500 mg every 4 to 6 hr. Maximum: 12,000 mg daily. Children over age 1 month. 25 mg/kg every 12 hr. Neonates. 10 mg/kg every 12 hr. To treat streptococcal pharyngitis , Children. 250 mg every 8 hr. To treat bone and joint infections, endocarditis, meningitis, and pericarditis caused by susceptible organisms
IV: Adults and adolescents. 1,500 to 2,000 mg every 4 to 6 hr. Maximum: 20,000 mg daily.
IV:,
I.M.INJECTION Children from birth to age 12. 10 to 20 mg/ kg every 4 hr or 20 to 40 mg/kg every 8 hr. For meningitis in neonates weighing up to 2 kg (4.4 lb), 25 to 50 mg/kg every 12 hr for first week after birth and then 50 mg/kg every 8 hr. For neonates weighing 2 kg or more, 50 mg/kg every 8 hr during first week after birth and then 50 mg/kg every 6 hr.

Mechanism of Action

Binds to certain penicillin-binding proteins in bacterial cell walls, thereby inhibiting the final stage of bacterial cell wall synthesis. The result is cell lysis. Nafcillin’s action is bolstered by its chemical composition; its unique side chain resists destruction by beta-lactamases.

Incompatibilities

Don’t mix nafcillin in same I.V. bag as aminoglycosides; they’re chemically incompatible.

Contraindications

Hypersensitivity to nafcillin, other penicillins, or their components

Interactions

aminoglycosides: Substantial mutual inactivation chloramphenicol, erythromycins, sulfonamides, tetracyclines: Possibly decreased therapeutic effects of nafcillin hepatotoxic : Increased risk of hepatotoxicity methotrexate: Increased risk of methotrexate toxicity probenecid: Increased blood nafcillin level all : Decreased nafcillin absorption

Side Efect

CNS: Depression, headache, seizures
EENT: Oral candidiasis
GI: Abdominal pain, diarrhea, nausea, pseudomembranous colitis, vomiting
GU: Vaginitis
HEME: Leukopenia, neutropenia
SKIN: Exfoliative dermatitis, pruritus, rash, urticaria
Other: Anaphylaxis; hypokalemia; injection site pain, redness, and swelling; serum sicknesslike reaction

Cautions

Obtain body fluid or tissue samples for culture and sensitivity testing, as prescribed, and obtain test results, if possible, before giving nafcillin, as ordered.

Give capsules or tablets at least 1 hour before meals or 2 hours afterward.

For I.M. injection, use only reconstituted solutions from vials. Inject deep into large muscle, preferably upper outer quadrant of gluteus maximus or lateral thigh.

For intermittent I.V. infusion, infuse over 30 to 60 minutes.

Give nafcillin at least 1 hour before or after aminoglycosides, especially if patient has renal disease.

When giving nafcillin to patient at risk for hypertension or fluid overload, be aware that each gram contains 2.5 mEq sodium.
WARNING Avoid giving nafcillin to premature neonate if drug was reconstituted with bacteriostatic water that contains benzyl alcohol. Doing so can cause potentially fatal metabolic acidosis and circulatory, CNS, renal, and respiratory dysfunction.

Monitor serum nafcillin level closely in children, as ordered, because liver and biliary tract, the main routes of nafcillin elimination, function immaturely in children.

Watch for evidence of superinfection, such as oral candidiasis and pseudomembranous colitis, especially in elderly, immunocompromised, or debilitated patients who receive large doses of nafcillin. If profuse, watery diarrhea develops, contact prescriber and expect to obtain a stool specimen to rule out pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold nafcillin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

PATIENT SAFTY

Instruct patient to take nafcillin capsules or tablets on an empty stomach.

Urge patient to complete entire prescription, even if she feels better.

Advise patient to notify prescriber if she experiences chills, fever, GI distress, or rash.

Urge patient to tell prescriber if diarrhea develops, even 2 or ore months after nafcillin therapy ends.

Category

Chemical class: Phenanthrene derivative
Therapeutic class: Analgesic, anesthesia adjunct

Pregnancy category: B

Indications

To relieve moderate to severe pain I.V., I.M., OR SUBCUTANEOUS INJECTION Adults weighing 70 kg (154 lb). 10 mg every 3 to 6 hr, p.r.n. Dosage adjusted for patients weighing more or less. As adjunct to anesthesia
I.V.INJECTION
Adults. 0.3 to 3 mg/kg over 10 to 15 min followed by 0.25 to 0.5 mg/kg, as needed.
DOSAGE ADJUSTMENT For patients who have repeatedly received an opioid agonist, initial dose possibly reduced to 25% of usual. For patients in whom tolerance to drug’s effects hasn’t developed, maximum usually is 20 mg/dose or 160 mg daily. Route Onset Peak Duration I.V. 2–3 min 30 min 3–4 hr I.M. In 15 min 1 hr 3–6 hr SubQ In 15 min Unknown 3–6 hr

Mechanism of Action

Binds with and stimulates mu and kappa opiate receptors in the spinal cord and higher levels in the CNS. In this way, nalbuphine alters the perception of and emotional response to pain.

Incompatibilities

Don’t give nalbuphine with diazepam or pentobarbital. Use separate I.V. line or flush line well before and after administration.

Contraindications

Hypersensitivity to nalbuphine or its components

Interactions

alfentanil, CNS depressants, fentanyl, sufentanil: Increased risk of hypotension and CNS and respiratory depression anticholinergics: Increased risk of severe constipation and urine retention antidiarrheals, such as difenoxin and atropine, loperamide, and paregoric: Increased risk of severe constipation and increased CNS depression antihypertensives: Increased risk of hypotension buprenorphine: Possibly decreased therapeutic effects of nalbuphine and increased risk of respiratory depression hydroxyzine: Increased risk of CNS depression and hypotension
MAO inhibitors: Risk of possibly fatal increased CNS excitation or depression metoclopramide: Possibly antagonized effects of metoclopramide naloxone,
naltrexone: Decreased pharmacologic effects of nalbuphine neuromuscular blockers: Increased risk of prolonged CNS and respiratory depression
alcohol use: Increased risk of coma, hypotension, profound sedation, and respiratory depression

Side Efect

CNS: Confusion, depression, dizziness, euphoria, fatigue, hallucinations, headache, nervousness, restlessness, seizures, syncope, tiredness, weakness
CV: Hypertension, hypotension, tachycardia
EENT: Blurred vision, diplopia, dry mouth
GI: Abdominal cramps, anorexia, constipation, nausea, vomiting
GU: Decreased urine output, ureteral spasm
RESP: Dyspnea, pulmonary edema, respiratory depression, wheezing
SKIN: Diaphoresis, flushing, pruritus, rash, sensation of warmth, urticaria
Other: Injection site burning, pain, redness, swelling, and warmth

Cautions

Use nalbuphine cautiously in patients taking other that can cause respiratory depression.

Keep resuscitation equipment and naloxone readily available to reverse nalbuphine’s effects, if needed.

For direct I.V. injection through an I.V. line with a compatible infusing solution, give drug slowly—no more than 10 mg over 3 to 5 minutes. Inject into free-flowing normal saline solution, D5W, or lactated Ringer’s solution.

During prolonged use, expect to give a stool softener to minimize constipation.

If patient is opioid-dependent, expect drug to cause withdrawal symptoms, such as abdominal cramps, anorexia, anxiety, backache, bone or joint pain, confusion, depression, diaphoresis, dysphoria, erythema, fear, fever, irritability, labile blood pressure and pulse, lacrimation, muscle spasms, myalgia, mydriasis, nasal congestion, nausea, opioid craving, piloerection, restlessness, rhinorrhea, sensation of crawling skin, sleep disturbances, tremor, uneasiness, vomiting, and yawning.
WARNING Be aware that drug may obscure neurologic assessment findings if patient has a cerebral aneurysm, head injury, or increased intracranial pressure.

PATIENT SAFTY

Advise patient to avoid hazardous activities until nalbuphine’s CNS effects are known.

Counsel patient against making important decisions while receiving drug because it may cloud her judgment.

Category

Chemical class: Naphthyridine derivative quinolone
Therapeutic class: Antibiotic

Pregnancy category: Not rated

(first trimester), B (later trimesters)

Indications

To treat UTI caused by gram-negative bacteria, such as most Enterobacter species, Escherichia coli, Klebsiella species, Morganella morganii, Proteus mirabilis, Proteus vulgaris, and Providencia rettgeri ORAL SUSPENSION, Adults and children age 12 and over. Initial: 1,000 mg every 6 hr for 1 to 2 wk. Maintenance: 500 mg every 6 hr. Maximum: 4,000 mg daily. Children ages 3 months to 12 years.Initial: 55 mg/kg daily in divided doses q.i.d. for 1 to 2 wk. Maintenance: 33 mg/kg daily in divided doses q.i.d.

Mechanism of Action

Inhibits the enzyme DNA gyrase, which is responsible for unwinding and supercoiling of bacterial DNA before it replicates. By inhibiting this enzyme, nalidixic acid causes bacterial cells to die.

Contraindications

Hypersensitivity to nalidixic acid or its components, porphyria, seizure disorder, use with melphalan or other related chemotherapeutic alkylating

Interactions

aluminum-, calcium-, and magnesium-containing antacids; didanosine; multivitamins containing iron or zinc; sucralfate: Possibly interference with nalidixic acid absorption chloramphenicol, nitrofurantoin, tetracycline: Decreased effects of nalidixic acid cyclosporine: Possibly increased blood cyclosporine level melphalan: Possibly increased risk of serious GI toxicity oral anticoagulants: Increased anticoagulant effects probenecid: Decreased effects of nalidixic acid and increased risk of

Side Efect

theophylline: Possibly increased blood theophylline level caffeine: Decreased clearance and prolonged half-life of caffeine

Side Efect

CNS: Confusion, drowsiness, hallucinations, headache, increased intracranial pressure with bulging fontanels (infants and children), light-headedness, malaise, paresthesia, peripheral neuropathy, psychosis, restlessness, seizures, tremor, weakness
EENT: Altered color perception, blurred vision, diplopia, halo vision, photophobia
GI: Abdominal pain, diarrhea, nausea, pseudomembranous colitis, vomiting
HEME: Eosinophilia, hemolytic anemia, leukopenia, thrombocytopenia
MS: Tendon rupture
SKIN: Jaundice, photosensitivity, pruritus, rash, Stevens-Johnson syndrome, urticaria
Other: Anaphylaxis, metabolic acidosis

Cautions

Be aware that nalidixic acid shouldn’t be given to patient with creatinine clearance below 10 ml/min/1.73 m2because of the increased risk of drug toxicity and should be used cautiously in patients with liver disease, epilepsy, glucose-6-phosphate dehydrogenase deficiency, or severe cerebral arteriosclerosis or renal failure.

Avoid giving drug within 2 hours of didanosine; multivitamins that contain iron or zinc; sucralfate; or antacid that contains aluminum, calcium, or magnesium.

If nalidixic acid therapy exceeds 2 weeks, monitor patient’s blood counts and renal and liver function test results periodically, as ordered.
WARNING Stop nalidixic acid at first sign of hypersensitivity, including rash, because it may indicate anaphylaxis. Reaction may occur with first dose. Expect to give epinephrine and supportive care.

If patient also takes cyclosporine or theophylline, monitor blood level of these and adjust dosage, as prescribed.

If patient has a history of seizures or cerebral arteriosclerosis, monitor for seizures during nalidixic acid therapy.

Notify prescriber if patient has symptoms of peripheral neuropathy (pain, burning, tingling, numbness, weakness, or altered sensations of light touch, pain, temperature, position sense, or vibration sense), which could be permanent; or tendon rupture, which requires immediate rest. In each case, expect to stop nalidixic acid.

PATIENT SAFTY

Encourage patient to drink plenty of fluids during therapy unless directed otherwise by prescriber.

Urge patient to complete entire course of therapy, even if she feels better before it’s finished.

Advise patient to protect skin from sunlight.

Urge patient to notify prescriber immediately about vision changes or such adverse CNS reactions as confusion, drowsiness, hallucinations, psychosis, and seizures.

Urge patient to stop drug and notify prescriber if rash or other evidence of hypersensitivity develops.

Tell patient to take drug at least 2 hours before or after aluminum-, calcium-, or magnesium-containing antacids; didanosine chewable buffered tablets or oral solution prepared from powder; multivitamins that contain iron or zinc; or sucralfate.

Caution patient to avoid hazardous tasks until CNS effects of drug are known.

Instruct patient to limit caffeine intake while taking nalidixic acid.

Tell patient to stop drug and notify prescriber if she develops tendon pain or inflammation or abnormal changes in motor or sensory function.

Urge patient to notify prescriber if diarrhea develops, even up to 2 months after nalidixic acid therapy stops.

Category

Chemical class: Thebaine derivative
Therapeutic class: Opioid antagonist

Pregnancy category: B

Indications

To treat known or suspected opioid overdose
I.V.INJECTION Adults and children age 5 and over weighing more than 20 kg (44 lb). 0.4 to 2 mg repeated every 2 to 3 min, p.r.n. If no response after 10 mg, patient may not have opioid-induced respiratory depression. Infants and children under age 5. 0.01 mg/kg as a single dose; if no improvement, another 0.1 mg/kg, as prescribed. Or, 0.1 mg/kg repeated every 2 to 3 min, as needed I.V., I.M., OR SUBCUTANEOUS INJECTION Neonates. 0.01 mg/kg repeated I.V. every 2 to 3 min, as prescribed, until desired response occurs. Or, initial I.V. dose of 0.1 mg/kg. To treat postoperative opioid-induced respiratory depression
I.V.INJECTION Adults and adolescents. Initial: 0.1 to 0.2 mg every 2 to 3 min until desired response occurs. Additional doses given every 1 to 2 hr, if needed, based on patient response. Children. Initial: 0.005 to 0.01 mg every 2 to 3 min until desired response occurs. Additional doses given every 1 to 2 hr, if needed, based on patient response. To reverse opioid-induced asphyxia I.V., I.M., OR SUBCUTANEOUS INJECTION Neonates. Initial: 0.01 mg/kg every 2 to 3 min until desired response occurs. Additional doses given every 1 to 2 hr, if needed, based on patient response. As adjunct to treat hypotension caused by septic shock
IV: OR INJECTION
Adults. 0.03 to 0.2 mg/kg over 5 min followed by continuous infusion of 0.03 to 0.3 mg/kg/hr for 1 to 24 hr, as needed, based on patient response. Route Onset Peak Duration I.V. 1–2 min 5–15 min 45 min or longer I.M., 2–5 min 5–15 min 45 min or SubQ longer

Mechanism of Action

Briefly and competitively antagonizes mu, kappa, and sigma receptors in the CNS, thus reversing analgesia, hypotension, respiratory depression, and sedation caused by most opioids. Mu receptors are responsible for analgesia, euphoria, miosis, and respiratory depression. Kappa receptors are responsible for analgesia and sedation. Sigma receptors control dysphoria and other delusional states.

Incompatibilities

Don’t mix naloxone with any other solution unless you verify the are compatible; drug is incompatible with alkaline, bisulfite, and metabisulfite solutions.

Contraindications

Hypersensitivity to naloxone or its components

Interactions

butorphanol, nalbuphine, pentazocine: Reversal of these ’ analgesic and adverse effects opioid analgesics: Reversal of these ’ analgesic and adverse effects, possibly withdrawal symptoms in opioid-dependent patients

Side Efect

CNS: Excitement, irritability, nervousness, restlessness, seizures, tremor, violent behavior
CV: Hypertension (severe), hypotension, ventricular fibrillation, ventricular tachycardia
GI: Nausea, vomiting
RESP: Pulmonary edema
SKIN: Diaphoresis
Other: Withdrawal symptoms

Cautions

Keep resuscitation equipment readily available during naloxone administration.

Administer drug by I.V. route whenever possible.

Give repeat doses as prescribed, depending on patient’s response.

Anticipate that rapid reversal of opioid effects can cause diaphoresis, nausea, and vomiting.
WARNING Watch for withdrawal symptoms, especially when giving naloxone to opioiddependent patient. Symptoms may include abdominal cramps, anorexia, anxiety, backache, bone or joint pain, confusion, depression, diaphoresis, dysphoria, erythema, fear, fever, irritability, labile blood pressure and pulse, lacrimation, muscle spasms, myalgia, mydriasis, nasal congestion, nausea, opioid craving, piloerection, restlessness, rhinorrhea, sensation of crawling skin, sleep disturbances, tremor, uneasiness, vomiting, and yawning.

Expect patient with hepatic or renal dysfunction to have increased circulating blood naloxone level.

PATIENT SAFTY

Inform patient or family that naloxone will reverse opioid-induced adverse reactions.

Urge opioid-dependent patient to seek drug rehabilitation.

Category

Chemical class: Thebaine derivative
Therapeutic class: Opioid antagonist

Pregnancy category: C

Indications

To treat opioid dependence
Adults. Initial: 25 mg, repeated within 1 hr, if needed and if no withdrawal symptoms occur. Maintenance: 50 to 150 mg daily or 350 mg/wk by intermittent dosing regimen. As adjunct to treat alcoholism
Adults. 50 mg daily (up to 100 mg daily for some patients) for 12 wk.
I.M.INJECTION
Adults. 380 mg every 4 wk or once monthly. naltrexone hydrochloride 716

Mechanism of Action

Displaces opioid agonists from—or blocks them from binding with—mu, kappa, and delta receptors. Opioid receptor blockade reverses the euphoric effect of opioids. Naltrexone also inhibits the effects of endogenous opioids, thus reducing alcohol craving. Route Onset Peak Duration P.O. 15–30 min In 12 hr 24 hr* I.M. Unknown 2 hr Unknown

Contraindications

Acute hepatitis, acute opioid withdrawal, concurrent use of opioid analgesics (including opioid agonists, such as methadone or levo-alpha-acetyl-methadol [LAAM]), failure of naloxone challenge test, hepatic failure, hypersensitivity to naltrexone or its components, opioid dependence, positive urine screen for opioids

Interactions

opioid analgesics: Reversal of analgesic and adverse effects of these , possibly withdrawal symptoms in opioid-dependent patients thioridazine: Increased somnolence and lethargy

Side Efect

CNS: Anxiety, chills, confusion, depression, dizziness, fatigue, fever, hallucinations, headache, insomnia, irritability, nervousness, restlessness, somnolence, suicidal ideation, syncope
CV: Chest pain, edema, hypertension, tachycardia
EENT: Blurred vision, burning eyes, conjunctivitis, dry mouth, eyelid swelling, hoarseness, pharyngitis, rhinitis, sneezing, tinnitus
GI: Abdominal cramps, anorexia, constipation, diarrhea, GI ulceration, hepatotoxicity with excessive doses, nausea, thirst, vomiting
GU: Difficult ejaculation, urinary frequency
MS: Arthralgia, back pain or stiffness, joint sitffness, muscle cramps, myalgia
RESP: Cough, dyspnea, eosinophilic pneumonia, upper respiratory tract infection
SKIN: Pruritus, rash
Other: Injection site reactions, such as pain, tenderness, induration, swelling, erythema, pruritus

Cautions

Use naltrexone cautiously in patients with severe renal impairment, thrombocytopenia, hemophilia, or severe hepatic failure.

To avoid withdrawal symptoms, wait 7 to 10 days after last opioid dose, as prescribed, before starting naltrexone. Because urine testing isn’t always conclusive, prepare patient for naloxone challenge test if there are any doubts about patient’s abstinence.

Give oral drug with food or antacids to decrease adverse GI reactions.

Dilute parenteral form using only diluent supplied in carton. Inject in gluteal muscle using only needle supplied in carton. Don’t substitute any components for components in carton. Store entire dose pack in refrigerator; unrefrigerated drug can be stored at room temperature for no more than 7 days.

Inspect injection site for reactions, such as tenderness, induration, swelling, or redness. Ask if patient feels pain or itching at the site. Report any such findings to prescriber because abscesses and site necrosis may occur and require surgical intervention.
WARNING Never give parenteral form intravenously.

Patients who receive naltrexone and need pain management are more likely to have longer, deeper respiratory depression and histamine-release reactions (such as facial swelling, itching, generalized erythema, and bronchoconstriction) if given an opioid analgesic. Expect alternative analgesics to be used, such as regional analgesia, conscious sedation with a benzodiazepine, nonopioid analgesics, or general anesthesia. If an opioid analgesic must be used, monitor patient closely.

Watch patient closely for suicidal tendencies throughout naltrexone therapy.

Anticipate that some patients may need treatment for up to 1 year.

PATIENT SAFTY

WARNING Caution patient against taking * For 50 mg; 48 hr for 100 mg; 72 hr for 150 mg. opioids during naltrexone therapy or in the future because she’ll be more sensitive to them. In fact, strongly warn patient that taking large doses of heroin or any other opioid (including methadone or LAAM) while taking naltrexone could lead to coma, serious injury, or death.

Explain that patient may have nausea after first injection but that it is usually mild and subsides within a few days. Most patients don’t have nausea with repeat doses.

Tell patient to report

Side Efect

promptly, especially dyspnea, coughing, wheezing, abdominal pain, and jaundice.

Urge family or caregiver to watch patient closely for abnormal behaviors, including suicidal tendencies, even after patient stops taking naltrexone.

Inform patient that naltrexone doesn’t eliminate or diminish alcohol withdrawal symptoms.

Urge patient to have comprehensive rehabilitation in addition to receiving naltrexone.

Inform patient about nonopioid treatments for cough, diarrhea, and pain.

Instruct patient to carry medical identification that lists naltrexone therapy.

Instruct women of childbearing age to notify prescriber if pregnancy is suspected.

Category

Chemical class: Propionic acid derivative
Therapeutic class: Analgesic, antiinflammatory, antipyretic

Pregnancy category: C

Indications

To relieve mild to moderate musculoskeletal inflammation, including ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis
Adults. 250 to 500 mg b.i.d. Maximum: 1,500 mg daily for limited periods, as prescribed. (NAPROXEN SODIUM)
Adults. 750 to 1,000 mg daily. Maximum: 1,500 mg daily.
Adults. 275 to 550 mg b.i.d. Maximum: 1,650 mg daily for limited periods, as prescribed.
Adults. 500 mg at bedtime in addition to daytime P.O. administration. Maximum: 1,500 mg daily (P.O. and suppository combined). To relieve symptoms of juvenile rheumatoid arthritis and other inflammatory conditions in children Children.10 mg/kg daily in divided doses b.i.d. To relieve symptoms of acute gouty arthritis
Adults. Initial: 750 mg, then 250 mg every 8 hr until symptoms subside.
Adults. Initial: 1,000 to 1,500 mg on day 1; then 1,000 mg daily until symptoms subside. Maximum: 1,500 mg daily.
Adults. Initial: 825 mg, then 275 mg every 8 hr until symptoms subside. To relieve mild to moderate pain, including acute tendinitis and bursitis, arthralgia, dysmenorrhea, and myalgia
Adults. Initial: 1,000 mg daily. Maximum: 1,500 mg daily.
Adults. Initial: 1,100 mg daily, increased as prescribed. Maximum: 1,500 mg daily.
Adults. Initial: 500 mg, then 250 mg every 6 to 8 hr, p.r.n. Maximum: 1,250 mg daily.
Adults. Initial: 550 mg, then 275 mg every 6 to 8 hr, p.r.n. Maximum: 1,375 mg daily. To relieve fever and mild to moderate musculoskeletal inflammation or pain
Adults. 220 mg every 8 to 12 hr; or 440 mg and 220 mg 12 hr later. Maximum: 660 mg daily for 10 days unless directed otherwise.
DOSAGE ADJUSTMENT For patients over age 65, 220 mg every 12 hr. Maximum: 440 mg for 10 days unless directed otherwise. Route Onset Peak Duration P.O. 1 hr 2–4 hr 7–12 hr (naproxen)* P.O. 30 min 1 hr 7–12 hr (naproxen sodium)*

Mechanism of Action

Blocks cyclooxygenase, the enzyme needed to synthesize prostaglandins, which mediate the inflammatory response and cause local vasodilation, swelling, and pain. Thus, naproxen, an NSAID, reduces symptoms of inflammation and relieves pain. Antipyretic action probably stems from effects on the hypothalamus, which increases peripheral blood flow, causing vasodilation and heat dissipation.

Contraindications

Angioedema, asthma, bronchospasm, nasal polyps, rhinitis, or urticaria induced by aspirin, iodides, or other NSAIDs; hypersensitivity to naproxen or its components

Interactions

ACE inhibitors: Decreased antihypertensive effects; increased risk of renal dysfunction acetaminophen: Increased risk of adverse renal effects with combined long-term use aluminum hydroxide or magnesium oxide antacids, cholestyramine, sucralfate: Possibly delayed absorption of naproxen anticoagulants, thrombolytics: Prolonged PT, increased risk of bleeding antihypertensives: Decreased effectiveness of antihypertensive aspirin: Decreased aspirin effectiveness from lowered plasma and peak aspirin levels
beta blockers: Decreased antihypertensive effects of these bone marrow depressants, such as aldesleukin and cisplatin: Increased risk of leukopenia and thrombocytopenia cefamandole, cefoperazone, cefotetan, plicamycin,
valproic acid: Increased risk of hypoprothrombinemia and bleeding
cimetidine: Altered blood naproxen level colchicine, glucocorticoids, other NSAIDs, potassium supplements, salicylates: Increased GI irritability and bleeding cyclosporine, gold compounds, nephrotoxic : Increased risk of nephrotoxicity digoxin: Increased blood digoxin level and risk of digitalis toxicity diuretics: Decreased diuretic effectiveness furosemide: Decreased natriuretic effect insulin, oral antidiabetic : Increased effectiveness of these ; risk of hypoglycemia lithium: Increased risk of lithium toxicity methotrexate: Increased risk of methotrexate toxicity naproxen-containing products: Increased risk of toxicity
phenytoin: Increased blood phenytoin level probenecid: Increased risk of naproxen toxicity alcohol use, smoking: Increased risk of naproxen-induced GI ulceration

Side Efect

CNS: Aseptic meningitis, chills, cognitive impairment, decreased concentration, depression, dizziness, dream disturbances, drowsiness, fever, headache, insomnia, light-headedness, malaise, seizures, stroke, vertigo
CV: Edema, heart failure, hypertension, MI, palpitations, tachycardia, vasculitis
EENT: Papilledema, papillitis, retrobulbar optic neuritis, stomatitis, tinnitus, vision or hearing changes
ENDO: Hyperglycemia, hypoglycemia
GI: Abdominal pain, anorexia, colitis, constipation, diarrhea, diverticulitis, dyspepsia, dysphagia, elevated liver function test results, esophagitis, flatulence, gastritis, gastroenteritis, gastroesophageal reflux disease, GI bleeding and ulceration, heartburn, hematemesis, hepatitis, indigestion, melena, nausea, pancreatitis, peptic ulceration, perforation of stomach or intestines, stomatitis, vomiting * For antirheumatism, onset is in 14 days, peak is unknown, and duration is 2 to 4 wk. For analgesia. For gout, 1 to 2 days.
GU: Elevated serum creatinine level, glomerulonephritis, hematuria, infertility (in women), interstitial nephritis, menstrual irregularities, nephrotic syndrome, renal failure, renal papillary necrosis
HEME: Agranulocytosis, anemia, aplastic anemia, eosinophilia, granulocytopenia, hemolytic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia
MS: Muscle weakness, myalgia
RESP: Asthma, dyspnea, eosinophilic pneumonitis, respiratory depression
SKIN: Alopecia, diaphoresis, ecchymosis, erythema multiforme, photosensitivity, pruritus, pseudoporphyria, purpura, rash, Stevens-Johnson syndrome, systemic lupus erythematosus, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, hyperkalemia

Cautions

Use naproxen with extreme caution in patients with a history of ulcer disease or GI bleeding because NSAIDs such as naproxen increase risk of GI bleeding and ulceration. Expect to use naproxen for the shortest time possible in these patients.

Serious GI tract ulceration, bleeding, and perforation may occur without
WARNING symptoms. Elderly patients are at greater risk. To minimize risk, give drug with food. If GI distress occurs, withhold drug and notify prescriber immediately.

Use naproxen cautiously in patients with hypertension, and monitor blood pressure closely. Drug may cause hypertension or worsen it. Because of naproxen’s sodium content, watch for fluid retention.

Rehydrate a dehydrated patient before giving drug. If patient has renal disease, monitor renal function closely during therapy.

Naproxen isn’t recommended for patients with advanced renal disease.
WARNING Monitor patient closely for thrombotic events, including MI and stroke, because NSAIDs increase the risk, especially if used in higher doses than recommended or for extended periods of time.

Monitor patient—especially if elderly or receiving long-term naproxen therapy— for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results because, in rare cases, elevations may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in elderly patients, patients taking diuretics or ACE inhibitors, and patients with heart failure, impaired renal function, or hepatic dysfunction; naproxen may cause renal failure.

Monitor CBC for decreased hemoglobin and hematocrit because drug may worsen anemia.
WARNING If patient has bone marrow suppression or is receiving treatment with an antineoplastic drug, monitor laboratory results (including WBC count), and watch for evidence of infection because antiinflammatory and antipyretic actions of naproxen may mask signs and symptoms, such as fever and pain.

Assess patient’s skin regularly for signs of rash or other hypersensitivity reaction because naproxen is an NSAID and may cause serious skin reactions without warning, even in patients with no history of NSAID sensivitity. At first sign of reaction, stop drug and notify prescriber.

Assess drug effectiveness in ankylosing spondylitis, as evidenced by decreased night pain, morning stiffness, and pain at rest; in osteoarthritis: decreased joint pain or tenderness and increased mobility, range of motion, and ability to perform daily activities; in rheumatoid arthritis: increased mobility and decreased joint swelling and morning stiffness; in acute gouty arthritis: decreased heat, pain, swelling, and tenderness in affected joints.

Tell prescriber if patient complains of vision changes; patient may need ophthalmic exam.

PATIENT SAFTY

Caution patient not to exceed recommended dosage, take for longer than directed, or take for more than 10 days without consulting prescriber because serious

Side Efect

may occur.

Tell patient to swallow delayed-release tabnaproxen 720 lets whole and not to break, crush, or chew them.

Advise patient to take drug with food to reduce GI distress.

Tell patient to take drug with a full glass of water and to remain upright for 15 to 30 minutes after taking it to prevent drug from lodging in esophagus and causing irritation.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Urge patient to keep scheduled appointments with prescriber to monitor progress.

Tell pregnant patient to avoid taking naproxen-containing products late in pregnancy.

Explain that naproxen may increase risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.

Inform patient that naproxen may increase risk of serious adverse GI reactions; stress the importance of seeking immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.

Alert patient to rare but serious skin reactions. Urge her to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity.

Advise patient to consult prescriber before taking naproxen-containing OTC products if he has asthma, ulcers, bleeding problems, high blood pressure, heart or kidney disease, a need for diuretic therapy, serious adverse effects from previous use of fever reducers or pain relievers, or persistent stomach problems, such as heartburn, upset stomach, or stomach pain.

Category

Chemical class: Selective serotonin 5-HT receptor agonist
Therapeutic class: Antimigraine

Pregnancy category: C

Indications

To relieve acute migraine with or without aura
Adults. 1 to 2.5 mg as a single dose, repeated in 4 hr p.r.n. if only partial relief obtained. Maximum: 5 mg daily.
DOSAGE ADJUSTMENT For patients with mild to moderate renal or hepatic impairment, maximum dosage reduced to 2.5 mg daily.

Mechanism of Action

Binds to receptors on intracranial blood vessels and sensory nerves in trigeminalvascular system to stimulate negative feedback, which halts serotonin release. Thus, naratriptan selectively constricts inflamed and dilated cranial vessels in the carotid circulation and inhibits production of proinflammatory neuropeptides.

Contraindications

Basilar or hemiplegic migraine; cerebrovascular, peripheral vascular, or coronary artery disease (ischemic or vasospastic); hypersensitivity to naratriptan or its components; hypertension (uncontrolled); severe hepatic or renal dysfunction; use within 24 hours of another 5-HT agonist or an ergotamine-containing or ergot-type drug, such as dihydroergotamine or methysergide

Interactions

ergot-containing : Possibly prolonged or additive vasospastic reactions fluoxetine, fluvoxamine, paroxetine, sertraline: Possibly weakness, hyperreflexia, and incoordination oral contraceptives: Possibly reduced clearance and increased blood level of naratriptan other selective serotonin 5-HT receptor agonists (including rizatriptan, sumatriptan, and zolmitriptan): Possibly additive effects

Side Efect

CNS: Dizziness, drowsiness, fatigue, malaise, paresthesia
CV: Chest pain, pressure, or heaviness
EENT: Decreased salivation, otitis media, pharyngitis, photophobia, rhinitis, throat tightness
GI: Nausea, vomiting

Cautions

WARNING Because naratriptan therapy can cause coronary artery vasospasm, monitor patient with coronary artery disease for signs or symptoms of angina while taking drug. Because naratriptan may also cause peripheral vasospastic reactions, such as ischemic bowel disease, monitor patient for abdominal pain and bloody diarrhea.

Monitor patient for hypertension during naratriptan therapy. It may increase systolic blood pressure by up to 32 mm Hg.

Be prepared to perform complete neurovascular assessment in any patient who reports an unusual headache or who fails to respond to first dose of naratriptan.

PATIENT SAFTY

Inform patient that naratriptan is used to treat acute migraine attacks and that it won’t prevent or reduce the number of migraines.

Advise patient not to take more than maximum prescribed amount during any 24-hour period.

If patient has no relief from initial dose of naratriptan, instruct her to notify prescriber rather than taking another dose in 4 hours because she may need a different drug.

Advise patient to seek reevaluation by prescriber if she has more than four headaches during any 30-day period while taking naratriptan.

Category

Chemical class: Recombinant humanized IgG4K monoclonal antibody
Therapeutic class: Anti-multiple sclerotic

Pregnancy category: C

Indications

To delay physical disability and reduce frequency of clinical exacerbations in relapsing forms of multiple sclerosis; to induce and maintain remission in moderately to severely active Crohn’s disease with evidence of inflammation in patients who had inadequate response to or are unable to tolerate conventional therapy and inhibitors of tumor necrosis factor alpha
IV:
Adults. 300 mg infused over 1 hr every 4 wk. Route Onset Peak Duration I.V. Unknown 24 wk Unknown

Mechanism of Action

Inhibits migration of leukocytes from vascular space, increasing the number of circulating leukocytes. It does this by binding to integrins on the surface of leukocytes (except neutrophils) and inhibiting adhesion of leukocytes to their counter receptors. In multiple sclerosis, lesions probably occur when activated inflammatory cells, including T-lymphocytes, cross the bloodbrain barrier.

Contraindications

History of or presence of progressive multifocal leukoencephalopathy, hypersensitivity to natalizumab or its components

Interactions

antineoplastics, immunosuppresants, immunomodulating agents: Increased risk of life-threatening infection

Side Efect

CNS: Depression, dizziness, fatigue, headache, progressive multifocal leukoencephalopathy (PML), rigors, somnolence, suicidal ideation, vertigo
CV: Chest discomfort, peripheral edema
EENT: Sinusutis, tonsillitis, tooth infection
GI: Abdominal discomfort, abnormal liver function test results, cholelithiasis, diarrhea, gastroenteritis, hepatotoxicity, jaindice, nausea
GU: Amenorrhea; dysmenorrhea; irregular menstruation; ovarian cysts; UTI; urinary incontinence, frequency, or urgency; vaginitis
MS: Arthralgia, back or limb pain, joint swelling, muscle cramp
RESP: Cough, pneumonia or other respiratory tract infection
SKIN: Dermatitis, night sweats, pruritus, rash, urticaria
Other: Acute hypersensitivity reaction, anaphylaxis, antibody formation, flulike illness, herpes, serious infection, weight gain or loss

Cautions

Make sure patient has enrolled in the TOUCH prescribing program before giving natalizumab. Once patient has signed and initialed the TOUCH program enrollment form, place original signed form in the patient’s medical record, send a copy to Biogen Idec, and give a copy to patient.

Be aware that all serious opportunistic and atypical infections must be reported to Biogen Idec at 1-800-456-2255 and the FDA’s MedWatch Program at 1-800-FDA1088.

Make sure patient with multiple sclerosis has had an MRI of the brain before starting natalizumab therapy. It will help distinguish evidence of multiple sclerosis from PML symptoms if they occur after therapy starts.

Dilute natalizumab concentrate 300 mg/ 15 ml in 100 ml of normal saline injection. Gently invert solution to mix completely. Do not shake.

Following dilution, infuse drug immediately over 1 hour. After infusion, flush line with normal saline injection.

Do not give natalizumab by I.V. push or bolus injection.

If not infused right away, refrigerate drug and use within 8 hours.

Observe patient during and for 1 hour after infusion for hypersensitivity reaction, evidenced by urticaria, dizziness, fever, rash, rigors, pruritus, nausea, flushing, hypotension, dyspnea, and chest pain. Reaction is more likely to occur if natalizumab therapy was interrupted. If hypersensitivity reaction occurs, notify prescriber; expect to withhold drug and provide supportive care.
WARNING Monitor patient closely for evidence of PML, a viral brain infection that may be disabling or fatal, because natalizumab increases the risk. If patient has unexplained neurologic changes, notify prescriber, withhold natalizumab, and prepare patient for a gadolinium-enhanced brain MRI and possible cerebrospinal fluid analysis, as ordered.

Expect that patient will be reevaluated 3 months after first infusion, 6 months after first infusion, and every 6 months thereafter.

Assess patient for evidence of infection because natalizumab may adversely affect immune system, increasing risk of infection. If infection occurs, expect to obtain appropriate specimens for culture and sensitivity and to treat accordingly.

Be aware that if patient with Crohn’s disease has no therapeutic response after 12 weeks, natalizumab should be discontinued. If patient is on chronic oral corticosteroid therapy, expect tapering of oral corticosteroid dose to begin. If patient can’t be tapered off oral corticosteroids within 6 months of starting natalizumab therapy, expect natalizumab to be discontinued. Likewise, if patient needs additional steroid use that extends beyond 3 months in a calendar year to control signs and symptoms of Crohn’s disease, expect natalizumab to be discontinued.

Assess patient’s liver function regularly, as ordered, because natalizumab may cause significant liver damage. Expect drug to be discontinued if patient becomes jaundiced or liver enzymes become elevated.

PATIENT SAFTY

Instruct patient on benefits and risks of natalizumab therapy, and provide medication guide for patient to read.

Encourage patient to ask questions before signing the enrollment form.

Emphasize need to report any worsening symptoms that persist over several days.

Tell patient to inform all health care providers that he is receiving natalizumab therapy.

Stress the need to have follow-up visits 3 months after first infusion, 6 months after first infusion, and at least every 6 months thereafter.

Instruct patient to report evidence of allergic reaction such as urticaria, dizziness, fever, rash, rigors, pruritus, nausea, flushing, hypotension, dyspnea, and chest pain.

Instruct patient to avoid people who have infections. Advise him to report fever, cough, lower-back or side pain, or other unexplained signs and symptoms because they may indicate infection.

Category

Chemical class: Amino acid derivative
Therapeutic class: Antidiabetic

Pregnancy category: C

Indications

To control blood glucose level in type 2 diabetes mellitus, either as monotherapy or with metformin or a thiazolidinedione
Adults. 120 mg t.i.d. 1 to 30 min before meals.
DOSAGE ADJUSTMENT Dosage reduced to 60 mg t.i.d. in patients with near-goal glycosylated hemoglobin (HbA1c) level.

Contraindications

Diabetic ketoacidosis, hypersensitivity to nateglinide or its components, type 1 diabetes mellitus Route Onset Peak Duration P.O. 20 min 1 hr 4 hr

Interactions

corticosteroids, sympathomimetics, thiazide diuretics, thyroid products: Possibly reduced hypoglycemic effects of nateglinide MAO inhibitors, nonselective beta-adrenergic blockers, NSAIDs, salicylates: Possibly additive hypoglycemic effects of nateglinide

Side Efect

CNS: Dizziness
ENDO: Hypoglycemia
GI: Cholestatic hepatitis, diarrhea, elevated liver enzyme levels, jaundice
MS: Accidental trauma, arthropathy, back pain
RESP: Bronchitis, cough, upper respiratory tract infection
SKIN: Pruritus, rash, urticaria
Other: Flulike symptoms ATP Inside beta cell Insulin Calcium channel Insulin secretion Outside beta cell Nateglinide ATP-potassium channel Ca++ Ca++ Ca++ K+ K+

Mechanism of Action

Nateglinide stimulates the release of insulin from functioning beta cells of the pancreas. In patients with type 2 diabetes mellitus, a lack of functioning beta cells diminishes blood levels of insulin and causes glucose intolerance. By interacting with the adenosine triphosphatase (ATP)–potassium channel on the beta cell membrane, nateglinide prevents potassium (K+) from leaving the cell. This causes the beta cell to depolarize and the cell membrane’s calcium channel to open. Consequently, calcium (Ca++) moves into the cell and insulin moves out of it. The extent of insulin release is glucose dependent; the lower the glucose level, the less insulin is secreted from the cell. By promoting insulin secretion in patients with type 2 diabetes mellitus, nateglinide improves glucose tolerance.

Cautions

Give nateglinide 1 to 30 minutes before meals to reduce the risk of hypoglycemia.

Monitor fasting glucose and HbA1clevels periodically, as ordered, to evaluate treatment effectiveness.

Monitor patient often in event of fever, infection, trauma, or surgery because transient loss of glucose control may occur, requiring an alteration in therapy.

PATIENT SAFTY

Instruct patient to take nateglinide 1 to 30 minutes before meals. Advise her to skip scheduled dose if she skips a meal to reduce the risk of hypoglycemia.

Teach patient to measure blood glucose level and recognize hyperglycemia and hypoglycemia. Advise her to notify prescriber if blood glucose level is abnormal.

Inform patient that strenuous exercise, insufficient calorie intake, and consumption of alcohol increase risk of hypoglycemia.

Advise patient to monitor blood glucose level as prescribed and to keep follow-up appointments to monitor HbA1clevel because drug may become less effective over time.

Category

Chemical class: Beta-adrenergic blocker
Therapeutic class: Antihypertensive

Pregnancy category: C

Indications

To treat hypertension
Adults. Initial: 5 mg once daily, increased at 2-wk intervals, as needed. Maximum: 40 mg once daily.
DOSAGE ADJUSTMENT For patients with moderate renal impairment (creatinine clearance less than 30 ml/min/1.73 m2) or moderate hepatic impairment (Child-Pugh Class B), initial dose reduced to 2.5 mg.

Mechanism of Action

May prevent arterial dilation and inhibit renin secretion, although precise mechanism of action isn’t known. Negative chronotropic effects may slow resting heart rate, and negative inotropic effects may reduce cardiac output, myocardial contractility, and myocardial oxygen consumption during stress or exercise. All of these actions may work together to lower systolic and diastolic blood pressure. Route Onset Peak Duration P.O. Unknown 1.5–4 hr Unknown

Contraindications

Advanced AV block, cardiogenic shock, decompensated cardiac failure, hypersensitivity to nebivolol or its components, sick sinus syndrome (unless permanent pacemaker is in place), severe bradycardia, severe hepatic impairment

Interactions

antiarrhythmias such as disopyramide, beta blockers, digoxin, diltiazem: Increased effect on AV conduction and myocardial depression; increased risk of bradycardia fluoxetine, paroxetine, propafenone, quinidine: Increased hypertensive effect of nebivolol guanethidine, reserpine: Possibly excessive reduction of sympathetic activity

Side Efect

CNS: Asthenia, dizziness, fatigue, headache, insomnia, paresthesia, somnolence, syncope, vertigo
CV: Allergic vasculitis, AV block, bradycardia, chest pain, hypercholesterolemia, hyperuricemia, MI, peripheral edema, peripheral ischemia, Raynaud’s phenomenon
GI: Abdominal pain, diarrhea, elevated liver enzymes, nausea, vomiting
GU: Acute renal failure, elevated BUN level, erectile dysfunction
HEME: Decreased platelet count, thrombocytopenia
RESP: Acute pulmonary edema, bronchospasm, dyspnea
SKIN: Pruritus, psoriasis, rash, urticaria
Other: Angioedema

Cautions

Know that patients with bronchospastic disease usually shouldn’t be treated with beta blocker therapy such as nebivolol.

Use nebivolol cautiously in patients with impaired hepatic or renal function.

Expect to administer an alpha blocker, as ordered, before starting nebivolol therapy in patients with pheochromocytoma.

Monitor blood pressure and pulse rate often, especially at start of nebivolol therapy and during
DOSAGE ADJUSTMENTs. Also monitor fluid intake and output and daily weight, and watch for evidence of heart failure, such as dyspnea, edema, fatigue, and jugular vein distention. If heart failure occurs or worsens, expect drug to be discontinued.

Be aware that drug shouldn’t be stopped abruptly because MI, myocardial ischemia, severe hypertension, or ventricular arrhythmias may result.

Expect to temporarily withhold nebivolol before surgery. If drug will be continued during perioperative period, monitor patient closely for protracted severe hypotension and difficulty restarting and keeping a heartbeat.

Assess distal circulation and peripheral pulses in patient with peripheral vascular disease because drug can worsen it.

Be aware that nebivolol may mask tachycardia from hyperthyroidism and that abrupt withdrawal can cause thyroid storm. Drug also can decrease blood glucose level, prolong or mask symptoms of hypoglycemia, and promote hyperglycemia in patient with diabetes mellitus; or worsen psoriasis.

Monitor patient closely for hypersensitivity reactions that may occur with beta blockers, especially patients with a history of severe anaphylactic reactions who may not be responsive to usual doses of epinephrine used to treat allergic reactions.

PATIENT SAFTY

Instruct patient to take nebivolol exactly as prescribed and not to stop abruptly.

Tell patient to weigh herself daily during nebivolol therapy and to notify prescriber if she gains more than 2 lb (0.9 kg) in 1 day or 5 lb. (2.3 kg) in 1 week.

Advise patient to rise slowly from a seated or lying position to minimize effects of orthostatic hypotension.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to contact prescriber about bleeding or bruising, cough at night, dizziness, edema, rash, shortness of breath, or slow pulse rate.

Advise diabetic patient to monitor her blood glucose level more often during nebivolol therapy because drug may mask symptoms of hypoglycemia.

Inform patient with psoriasis that drug may aggravate this condition.

Category

Chemical class: Phenylpiperazine derivative
Therapeutic class: Antidepressant

Pregnancy category: C

Indications

To treat major depression
Adults. Initial: 100 mg b.i.d., increased by 100 to 200 mg daily every wk, as prescribed. Maintenance: 150 to 300 mg b.i.d. Maximum: 600 mg daily.
DOSAGE ADJUSTMENT Initial dosage possibly reduced to 50 mg b.i.d. for elderly or debilitated patients; then dosage adjusted as ordered, based on patient response. Route Onset Peak Duration P.O. Several wk Unknown Unknown

Mechanism of Action

May inhibit serotonin reuptake at presynaptic neurons, which may increase neuronal level of serotonin, an inhibitory neurotransmitter thought to regulate mood. Nefazodone also may act as a postsynaptic serotonin receptor antagonist, further increasing the amount of synaptic serotonin that’s available.

Contraindications

Concurrent use of astemizole, cisapride, or terfenadine; hypersensitivity to nefazodone, other phenylpiperazine antidepressants, or their components; restarting nefazodone therapy that was discontinued because of nefazodone hydrochloride 726 liver injury; use within 14 days of MAO inhibitor therapy

Interactions

alprazolam, buspirone, carbamazepine, cyclosporine, modafinil, triazolam: Increased blood levels of these antihypertensives: Increased risk of hypotension astemizole, cisapride, terfenadine: Increased blood levels of these , prolonged QT interval, and, possibly, serious cardiovascular effects, including death from ventricular tachycardia cilostazol: Decreased cilostazol clearance, increased adverse effects of cilostazol, such as headache dextromethorphan, sibutramine, tramadol, trazodone: Increased risk of serotonin syndrome digoxin: Increased blood digoxin level, increased risk of digitalis toxicity
haloperidol: Decreased haloperidol clearance indinavir: Inhibited indinavir metabolism levobupivacaine: Increased blood levobupivacaine level, possibly toxicity lovastatin, simvastatin: Increased risk of rhabdomyolysis and myositis
MAO inhibitors: Possibly fatal reactions, including autonomic instability (with rapidly fluctuating vital signs), hyperthermia, mental status changes (such as severe agitation progressing to delirium and coma), muscle rigidity, and myoclonus methadone: Increased blood level and adverse effects of methadone, additive CNS effects
nevirapine: Increased nefazodone metabolism, inhibited nevirapine metabolism ritonavir: Inhibited nefazodone and ritonavir metabolism
sildenafil: Decreased sildenafil clearance tacrolimus: Decreased tacrolimus clearance and increased adverse effects, including delirium and renal failure
alcohol use: Increased risk of CNS depression

Side Efect

CNS: Abnormal gait, apathy, asthenia, ataxia, chills, confusion, decreased concentration, delusions, depersonalization, dizziness, dream disturbances, euphoria, fever, hallucinations, headache, hostility, hypotonia, insomnia, light-headedness, malaise, memory loss, myoclonic jerks, neuralgia, paranoia, paresthesia, somnolence, suicidal ideation, syncope, tremor, vertigo
CV: Angina, hypertension, hypotension, peripheral edema, orthostatic hypotension, tachycardia, vasodilation, ventricular arrhythmias
EENT: Abnormal vision, blurred vision, conjunctivitis, diplopia, dry eyes and mouth, earache, epistaxis, eye pain, gingivitis, halitosis, hyperacusis, laryngitis, mydriasis, neck rigidity, periodontal abscess, pharyngitis, photophobia, stomatitis, taste perversion, tinnitus, visual field defects
ENDO: Breast pain, gynecomastia, lymphadenopathy
GI: Abdominal distention, colitis, constipation, diarrhea, elevated liver function test results, eructation, esophagitis, gastritis, gastroenteritis, hernia, hepatotoxicity, hiccups, increased appetite, indigestion, lifethreatening hepatic failure, nausea, peptic ulcer, rectal bleeding, thirst, vomiting
GU: Abnormal ejaculation; amenorrhea; cystitis; hematuria; hypermenorrhea; impotence; libido changes; nocturia; pelvic pain; polyuria; renal calculi; urinary frequency, incontinence, or urgency; urine retention; UTI; vaginal bleeding; vaginitis
HEME: Anemia, leukopenia
MS: Arthralgia, arthritis, bursitis, dysarthria, gout, muscle stiffness, tenosynovitis
RESP: Asthma, bronchitis, cough, dyspnea, pneumonia
SKIN: Acne, alopecia, dry skin, ecchymosis, eczema, maculopapular rash, photosensitivity, pruritus, rash, urticaria
Other: Allergic reaction, dehydration, infection, serotonin syndrome, weight loss

Cautions

WARNING Be aware that nefazodone should not be given with astemizole, cisapride, MAO inhibitors, or terfenadine; serious, even fatal, reactions may occur.
WARNING Be aware that life-threatening hepatic failure has occurred during nefazodone therapy, resulting in need for transplant or even death. Monitor patient for signs of hepatic failure, such as jaundice, malaise, and elevated liver function test results.

Assess for evidence of serotonin syndrome, such as abdominal cramps, aggression, agitation, chills, diarrhea, headache, insomnia, lack of coordination, nausea, palpitations, paresthesia, poor concentration, and worsening of obsessive thoughts.

Monitor patient closely for suicidal tendencies, especially when therapy starts or dosage changes, because depression may worsen temporarily. Follow facility policy.

PATIENT SAFTY

Instruct patient to take nefazodone exactly as prescribed and not to alter dosage.

Urge patient to immediately report evidence of hepatic failure, such as jaundice, dark urine, lack of appetite, nausea, or abdominal pain.

Inform patient that antidepressant effects may not occur for several weeks and that treatment may last 6 months or longer.

Caution patient to avoid alcohol during nefazodone therapy.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Suggest that patient try sugarless gum or hard candy for dry mouth. Urge her to notify prescriber if dry mouth persists.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes.

Category

Chemical class: Aminoglycoside
Therapeutic class: Antibiotic

Pregnancy category: D

Indications

To suppress intestinal bacterial growth in preoperative bowel preparation (24-HR REGIMEN)
Adults. 1 g every hr for 4 doses and then 1 g every 4 hr for remainder of 24 hr before surgery. Or, for 8 a.m. surgery, 1 g of neomycin with erythromycin at 1 p.m., 2 p.m., and 11 p.m. the day before surgery. Children. 25 mg/kg at 1 p.m., 2 p.m., and 11 p.m. the day before surgery. (2TO3-DAY REGIMEN) Adults and children. 88 mg/kg every 4 hr in 6 equally divided doses for 2 to 3 days before surgery. As adjunct in hepatic encephalopathy
Adults. 4 to 12 g daily in divided doses every 6 hr for 5 to 6 days. Children.50 to 100 mg/kg daily in divided doses every 6 hr for 5 to 6 days. To treat infectious diarrhea caused by enteropathic Escherichia coli Adults and children.50 mg/kg daily in divided doses q.i.d. for 2 to 3 days.

Mechanism of Action

Is transported into bacterial cells, where it competes with messenger RNA to bind with a specific receptor protein on the 30S ribosomal subunit of DNA. This action causes abnormal, nonfunctioning proteins to form. A lack of functional proteins causes bacterial cell death.

Contraindications

Hypersensitivity or serious reaction to neomycin, other aminoglycosides, or their components; inflammatory or ulcerative GI disease; intestinal obstruction

Interactions

digoxin, spironolactone: Possibly reduced absorption rate of these dimenhydrinate: Possibly masked symptoms of neomycin-induced ototoxicity methotrexate: Possibly decreased absorption and bioavailability of methotrexate neuromuscular blockers: Potentiated neuromuscular blockade, increased risk of prolonged respiratory depression oral anticoagulants: Possibly potentiated anticoagulant effects

Side Efect

EENT: Ototoxicity
GI: Diarrhea, malabsorption syndrome (decreased serum carotene level and xylose absorption, increased fecal fat and flatulence), nausea, pseudomembranous colitis, vomiting
GU: Nephrotoxicity

Cautions

Monitor patient’s BUN and serum creatineomycin sulfate 728 nine levels to assess renal function before and during neomycin therapy. Expect to decrease dosage or stop drug if nephrotoxicity develops.

Monitor blood neomycin level, as directed, to assess for therapeutic range of 5 to 10 mcg/ml.
WARNING Neomycin is highly ototoxic and may cause hearing loss and tinnitus.

Watch for evidence of pseudomembranous colitis, such as severe abdominal cramps and severe, watery diarrhea.

Anticipate that neomycin’s curare-like effect may worsen muscle weakness in patients with neuromuscular disorders, such as myasthenia gravis and parkinsonism.

PATIENT SAFTY

Urge patient to complete full course of neomycin therapy.

Unless contraindicated, urge patient to drink plenty of fluids to prevent nephrotoxicity.

Urge patient undergoing bowel preparation to comply with recommended regimen, including low-residue diet, bisacodyl enema administration, and neomycin use.

Advise patient to notify prescriber about hearing loss or ringing in ears.

Category

Chemical class: Quaternary ammonium compound
Therapeutic class: Anticholinesterase, curare antidote

Pregnancy category: C

Indications

To treat symptoms of myasthenia gravis
Adults. Initial: 15 mg every 3 to 4 hr. Dosage adjusted based on clinical response. Maintenance: 150 mg daily in divided doses based on clinical response. Children.2 mg/kg daily in 6 to 8 divided doses. I.M.
Adults. Initial: 0.5 mg. Dosage adjusted based on clinical response. Children.0.01 to 0.04 mg/kg every 2 to 3 hr. To reverse nondepolarizing neuromuscular blockade
I.V.INJECTION
Adults. 0.5 to 2 mg by slow push, repeated as needed up to 5 mg; 0.6 to 1.2 mg of atropine or 0.2 to 0.6 mg of glycopyrrolate given with or a few minutes before neostigmine, as ordered. Children. 0.04 mg/kg by slow push; 0.02 mg of atropine/kg is given I.M. or subcutaneously with each dose or alternate doses. To prevent postoperative, nonobstructive urine retention and abdominal distention (adynamic ileus) I.M.OR SUBCUTANEOUS INJECTION
Adults. 0.25 mg immediately after surgery and repeated every 4 to 6 hr for 2 to 3 days. To treat postoperative, nonobstructive urine retention and abdominal distention (adynamic ileus) I.M. OR SUBCUTANEOUS INJECTION (
Adults. 0.5 mg; injections repeated every 3 hr for at least 5 doses if patient has voided or bladder has emptied within 1 hr. Route Onset Peak Duration P.O. 45 –75 min* Unknown 3–6 hr I.V. 4 –8 min 30 min 2–4 hr I.M. 20–30 min30 min 2–4 hr

Mechanism of Action

Inhibits action of cholinesterase, an enzyme that destroys acetylcholine at myoneuronal junctions, thereby increasing acetylcholine accumulation at myoneuronal junctions and facilitating nerve impulse transmission across the junctions. This action:

helps prevent or relieve urine retention by increasing detrusor muscle tone in the bladder and causing bladder contractions strong enough to induce urination * For adynamic ileus, 2 to 4 hr. For adynamic ileus, 10 to 30 min.

prevents or treats postoperative abdominal distention by increasing gastric motility and tone

improves muscle strength and increases muscle response to repetitive nerve stimulation in myasthenia gravis.

Contraindications

Hypersensitivity to neostigmine, other anticholinesterases, bromides, or their components; mechanical obstruction of intestinal or urinary tract; peritonitis

Interactions

aminoglycosides, anesthetics, capreomycin, colistimethate, colistin, lidocaine, lincomycins, polymyxin B, quinine: Increased risk of neuromuscular blockade anticholinergics: Possibly masked signs of cholinergic crisis guanadrel, guanethidine, mecamylamine, trimethaphan: Possibly antagonized effects of neostigmine, possibly decreased antihypertensive effects neuromuscular blockers: Possibly prolonged action of depolarizing—and antagonized action of nondepolarizing—neuromuscular blockers procainamide,
quinidine: Possibly antagonized effects of neostigmine quinine: Decreased neostigmine effectiveness

Side Efect

CNS: Dizziness, drowsiness, headache, seizures, syncope, weakness
CV: Arrhythmias (AV block, bradycardia, nodal rhythm, tachycardia), cardiac arrest, ECG changes, hypotension
EENT: Increased salivation, lacrimation, miosis, vision changes
GI: Abdominal cramps, diarrhea, flatulence, increased peristalsis, nausea, vomiting
GU: Urinary frequency
MS: Arthralgia, dysarthria, muscle spasms
RESP: Bronchospasm, dyspnea, increased bronchial secretions, respiratory arrest or depression
SKIN: Flushing, diaphoresis, rash, urticaria

Cautions

Be aware that 15 mg oral neostigmine bromide is equivalent to 0.5 mg parenteral neostigmine methylsulfate.

If also giving atropine, be sure to administer it before neostigmine, as prescribed.

When giving neostigmine I.V., make sure patient is well ventilated and airway remains patent until normal respiration is assured.

If patient has myasthenia gravis, give drug night and day, as ordered, with larger portions of daily dose during periods of increased fatigue. If patient’s condition becomes refractory to neostigmine, expect to reduce dosage or discontinue drug, as prescribed, for a few days.
WARNING Monitor patient for evidence of neostigmine overdose, which can cause possibly fatal cholinergic crisis (increased muscle weakness, including respiratory muscles). Expect to stop neostigmine and atropine, as ordered.

PATIENT SAFTY

Instruct patient to take neostigmine exactly as prescribed.

Advise patient to take drug with food or milk to reduce adverse GI reactions.

Suggest that patient with myasthenia gravis keep a daily record of doses and

Side Efect

during therapy.

Instruct patient to schedule activities to minimize fatigue.

Category

Chemical class: Human B-type natriuretic peptide
Therapeutic class: Arterial and venous smooth muscle cell relaxant

Pregnancy category: C

Indications

To reduce dyspnea at rest or with minimal activity in patients with acute decompensated congestive heart failure
IV:,
I.V.INJECTION
Adults. 2-mcg/kg bolus and then continuous infusion of 0.01 mcg/kg/min for up to 48 hr. Route Onset Peak Duration I.V. In 15 min 1 hr 3 hr

Mechanism of Action

Binds to guanylate cyclase receptor of vasnesiritide 730 cular smooth muscle and endothelial cells. This action increases intracellular levels of cyclic guanosine monophosphate, which leads to arterial and venous smooth muscle cell relaxation. Ultimately, nesiritide reduces pulmonary capillary wedge pressure and systemic arterial pressure in patients with congestive heart failure, which decreases the heart’s workload and subsequently relieves dyspnea.

Incompatibilities

Don’t infuse nesiritide through same I.V. line as bumetanide, enalaprilat, ethacrynate sodium, furosemide, heparin, hydralazine, or insulin because these are chemically and physically incompatible with nesiritide. Don’t infuse that contain the preservative sodium metabisulfite through same I.V. line as nesiritide.

Contraindications

Hypersensitivity to nesiritide or its components; primary therapy for cardiogenic shock; systolic blood pressure less of than 90 mm Hg

Interactions

ACE inhibitors: Increased risk of symptomatic hypotension

Side Efect

CNS: Anxiety, dizziness, headache, insomnia
CV: Angina, bradycardia, hypotension, PVCs, ventricular tachycardia
GI: Abdominal pain, nausea, vomiting
GU: Elevated serum creatinine level
MS: Back pain

Cautions

WARNING Be aware that nesiritide isn’t recommended for patients suspected to have low cardiac filling pressures or patients for whom vasodilating aren’t appropriate, such as those with constrictive pericarditis, pericardial tamponade, restrictive or obstructive cardiomyopathy, significant valvular stenosis, or other conditions in which cardiac output depends on venous return.

Reconstitute 1.5-mg vial by adding 5 ml diluent removed from a 250-ml plastic I.V. bag containing preservative-free D5W, normal saline solution, dextrose 5% in half-normal (0.45) saline solution, or dextrose 5% in quarter-normal (0.2) saline solution.

Don’t shake vial. Rock it gently so all surfaces, including the stopper, are in contact with diluent to ensure complete reconstitution. Inspect drug for particulate matter and discoloration; if present, discard drug.

Withdraw entire contents of reconstituted solution and add it to 250-ml plastic I.V. bag used to withdraw diluent to yield a solution of about 6 mcg/ml. Invert I.V. bag several times to ensure complete mixing.

After preparing infusion bag, withdraw bolus volume from infusion bag and give it over about 60 seconds. Immediately after bolus, infuse drug at 0.1 ml/kg/hr, which will deliver 0.01 mcg/kg/min.

Prime I.V. tubing with 25 ml of solution before connecting to the I.V. line and before administering the bolus dose or starting the infusion.

Flush the I.V. line between doses of nesiritide and incompatible .

Because nesiritide binds to heparin and therefore could bind to the heparin lining of a heparin-coated catheter, don’t give it through a central heparin-coated catheter.

Store reconstituted vials at room temperature (20° to 25° C [68° to 77° F]) or refrigerate (2° to 8° C [36° to 46° F]) for up to 24 hours.

Because nesiritide contains no antimicrobial preservatives, discard the reconstituted solution after 24 hours.

Monitor blood pressure and heart rate and rhythm frequently during therapy.

If hypotension occurs, notify prescriber and expect to reduce dosage or discontinued the drug. Implement measures to support blood pressure as prescribed.

Assess patient’s breath sounds and respiratory rate, rhythm, depth, and quality frequently during drug therapy.

Monitor serum creatinine level during drug therapy and notify prescriber of abnormal results.

Store unopened drug at controlled room temperature or refrigerate. Keep in carton until time of use.

PATIENT SAFTY

Instruct patient to notify you or another nurse if she becomes dizzy because this may indicate hypotension.

Reassure patient that her blood pressure, heart rate, and breathing will be monitored frequently.

Category

Chemical class: Aminoglycoside
Therapeutic class: Antibiotic

Pregnancy category: D

Indications

To treat serious systemic infections, such as intra-abdominal infections, lower respiratory tract infections, septicemia, and skin and soft-tissue infections, caused by Enterobacter aerogenes, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Serratia species, and Staphylococcus aureus
IV:,
I.M.INJECTION Adults and children age 12 and over.1.3 to 2.2 mg/kg every 8 hr or 2 to 3.25 mg/kg every 12 hr for 7 to 14 days. Maximum: 7.5 mg/kg daily. Children ages 6 weeks to 12 years. 1.8 to 2.7 mg/kg every 8 hr or 2.7 to 4 mg/kg every 12 hr for 7 to 14 days. Infants up to age 6 weeks.2 to 3.25 mg/kg every 12 hr for 7 to 14 days. To treat complicated UTI caused by Citrobacter species, Enterobacter species, E. coli, K. pneumoniae, P. mirabilis, P. aeruginosa, Serratia species, and Staphylococcus species
IV:,
I.M.INJECTION Adults and adolescents. 1.5 to 2 mg/kg every 12 hr for 7 to 14 days. Maximum: 7.5 mg/kg daily.

Mechanism of Action

Is transported into bacterial cells, where it competes with messenger RNA to bind with a specific receptor protein on the 30S ribosomal subunit of DNA. This action causes abnormal, nonfunctioning proteins to form. A lack of functional proteins causes bacterial cell death.

Incompatibilities

Don’t mix netilmicin with beta-lactam antibiotics (penicillins and cephalosporins) because substantial mutual inactivation may result. If prescribed concurrently, administer these at separate sites.

Contraindications

Hypersensitivity to netilmicin, other aminoglycosides, or their components

Interactions

capreomycin, other aminoglycosides: Increased risk of nephrotoxicity, neuromuscular blockade, and ototoxicity cephalosporins, nephrotoxic : Increased risk of nephrotoxicity loop diuretics, ototoxic : Increased risk of ototoxicity methoxyflurane, polymyxins (parenteral): Increased risk of nephrotoxicity and neuromuscular blockade neuromuscular blockers: Increased neuromuscular blockade

Side Efect

CNS: Disorientation, dizziness, encephalopathy, headache, myasthenia gravis–like syndrome, neuromuscular blockade (acute muscle paralysis and apnea), paresthesia, peripheral neuropathy, seizures, vertigo, weakness
CV: Hypotension, palpitations
EENT: Blurred vision, hearing loss, nystagmus, tinnitus
GI: Diarrhea, elevated liver function tests results, nausea, vomiting
GU: Elevated BUN and serum creatinine levels, nephrotoxicity, oliguria, proteinuria
HEME: Anemia, eosinophilia, leukopenia, prolonged PT, thrombocytopenia, thrombocytosis
MS: Muscle twitching
RESP: Apnea
SKIN: Allergic dermatitis, erythema, pruritus, rash
Other: Angioedema; hyperkalemia; injection site hematoma, induration, and pain

Cautions

To prepare netilmicin for I.V. use, dilute each dose in 50 to 200 ml of suitable diluent, such as normal saline solution, D5W, or lactated Ringer’s solution, and give slowly over 30 to 60 minutes.

Ensure adequate hydration during therapy to maintain adequate renal function. netilmicin sulfate 732

Monitor blood netilmicin level; optimum peak level is 6 to 10 mcg/ml and trough level is 0.5 to 2 mcg/ml.

Check patient’s BUN and serum creatinine levels, urine specific gravity, and creatinine clearance during netilmicin therapy, as ordered.

Anticipate higher risk of nephrotoxicity in elderly patients, those with impaired renal function, and those who receive high doses or prolonged netilmicin therapy.

Reduce dosage or discontinue drug, as ordered, if signs of drug-induced auditory or vestibular toxicity develop; the damage may be permanent.

PATIENT SAFTY

Encourage patient to drink plenty of fluids during netilmicin therapy.

Instruct patient to notify prescriber immediately about dizziness, hearing loss, muscle twitching, nausea, numbness and tingling, ringing or buzzing in ears, seizures, significant changes in amount of urine or frequency of urination, and vomiting.

Urge patient to keep follow-up appointments to monitor progress.

Category

Chemical class: Dihydropyridine derivative
Therapeutic class: Antianginal, antihypertensive

Pregnancy category: C

Indications

To manage angina pectoris and Prinzmetal’s angina, to manage hypertension Adults and adolescents. 20 to 40 mg t.i.d., increased every 3 days, as prescribed.
Adults. 30 mg b.i.d.
IV:
Adults. 0.5 to 2.2 mg/hr by continuous infusion. To control acute hypertension
IV:
Adults. Initial: 5 mg/hr by continuous infusion; increased by 2.5 mg/hr every 5 to 15 min, as prescribed. Maximum: 15 mg/hr. Route Onset Peak Duration P.O. 20 min 1–2 hr Unknown P.O. () 20 min 1–2 hr 12 hr I.V. Immediate Unknown Unknown

Mechanism of Action

May slow extracellular calcium movement into myocardial and vascular smoothmuscle cells by deforming calcium channels in cell membranes, inhibiting ioncontrolled gating mechanisms, and interfering with calcium release from the sarcoplasmic reticulum. By decreasing the intracellular calcium level, nicardipine inhibits smooth-muscle cell contraction and dilates coronary and systemic arteries. As with other calcium channel blockers, these actions lead to decreased myocardial oxygen requirements and reduced peripheral resistance, blood pressure, and afterload.

Incompatibilities

Don’t mix nicardipine with sodium bicarbonate or LR solution, and don’t administer through same I.V. line.

Contraindications

Advanced aortic stenosis, hypersensitivity to any calcium channel blocker, secondor third-degree AV block in patient without artificial pacemaker

Interactions

anesthetics (hydrocarbon inhalation): Possibly hypotension beta blockers, other antihypertensives, prazocin: Increased risk of hypotension calcium supplements: Possibly impaired action of nicardipine
cimetidine: Increased nicardipine bioavailability digoxin: Transiently increased blood digoxin level, increased risk of digitalis toxicity disopyramide, flecainide: Increased risk of bradycardia, conduction defects, and heart failure estrogens: Possibly increased fluid retention and decreased therapeutic effects of nicardipine lithium: Increased risk of neurotoxicity NSAIDs, sympathomimetics: Possibly decreased therapeutic effects of nicardipine procainamide,
quinidine: Possibly prolonged QT interval grapefruit, grapefruit juice: Possibly increased bioavailability of nicardipine high-fat meals: Decreased blood nicardipine level
alcohol use: Increased hypotensive effect

Side Efect

CNS: Anxiety, asthenia, ataxia, confusion, dizziness, drowsiness, headache, nervousness, paresthesia, psychiatric disturbance, syncope, tremor, weakness
CV: Arrhythmias (bradycardia, tachycardia), chest pain, heart failure, hypotension, orthostatic hypotension, palpitations, peripheral edema
EENT: Altered taste, blurred vision, dry mouth, epistaxis, gingival hyperplasia, pharyngitis, rhinitis, tinnitus
ENDO: Gynecomastia, hyperglycemia
GI: Anorexia, constipation, diarrhea, elevated liver function test results, indigestion, nausea, thirst, vomiting
GU: Dysuria, nocturia, polyuria, sexual dysfunction, urinary frequency
HEME: Anemia, leukopenia, thrombocytopenia
MS: Joint stiffness, muscle spasms
RESP: Bronchitis, cough, upper respiratory tract infection
SKIN: Dermatitis, diaphoresis, erythema multiforme, flushing, photosensitivity, pruritus, rash, Stevens-Johnson syndrome, urticaria
Other: Hypokalemia, injection site irritation, weight gain

Cautions

Check blood pressure and pulse rate before nicardipine therapy begins, during dosage changes, and periodically throughout therapy. During prolonged therapy, periodically assess ECG tracings for arrhythmias and other changes.

Dilute each 25-mg ampule of nicardipine with 240 ml of solution to yield 0.1 mg/ ml. Mixture is stable at room temperature for 24 hours.

If using premixed nicardipine for intravenous infusion, check strength carefully because drug comes as single strength (20 mg nicardipine in 200 ml of solution, providing 0.1 mg/ml) or double strength (40 mg nicardipine in 200 ml of solution, providing 0.2 mg/ml).

Administer continuous infusion by I.V. pump or controller, and adjust according to patient’s blood pressure, as prescribed.

Change peripheral I.V. site every 12 hours, if feasible, to minimize peripheral venous irritation.

Give first dose of oral nicardipine 1 hour before stopping I.V. infusion, as ordered.

Monitor fluid intake and output and daily weight for signs of fluid retention, which may precipitate heart failure. Also assess for signs of heart failure, such as crackles, dyspnea, jugular vein distention, peripheral edema, and weight gain.

During prolonged therapy, periodically monitor liver and renal function test results. Expect elevated liver function test results to return to normal after drug is discontinued.

Monitor serum potassium level during prolonged therapy. Hypokalemia increases the risk of arrhythmias.

Because of drug’s negative inotropic effect on some patients, closely monitor patients who take a beta blocker or have heart failure or significant left ventricular dysfunction.
WARNING Expect to taper dosage gradually before discontinuing drug. Otherwise, angina or dangerously high blood pressure could result.

PATIENT SAFTY

Urge patient to take nicardipine as prescribed, even if she feels well.

Instruct patient to swallow capsules whole, not to chew, crush, cut, or open them.

Advise patient not to take drug within 1 hour of eating a high-fat meal or grapefruit product. Urge her not to alter the amount of grapefruit products in her diet without consulting prescriber.
WARNING Caution patient against stopping nicardipine abruptly because angina or dangerously high blood pressure could result.

Teach patient how to take her pulse, and urge her to notify prescriber immediately if it falls below 50 beats/minute.

Teach patient how to measure blood pressure, and urge her to do so weekly if drug was prescribed for hypertension. Suggest that she keep a log of blood pressure readings and take it to follow-up visits.

Advise patient to change position slowly to minimize orthostatic hypotension.

Urge patient to avoid potentially hazardous activities until drug’s CNS effects are known.

Advise patient to notify prescriber immediately about chest pain that’s not relieved by rest or nitroglycerin, constipation, irregular heartbeats, nausea, pronounced dizziness, severe or persistent headache, and swelling of hands or feet.

Encourage patient to comply with suggested lifestyle changes, such as alcohol moderation, low-sodium or low-fat diet, regular exercise, smoking cessation, stress management, and weight reduction.

Inform patient that saunas, hot tubs, and prolonged hot showers may cause dizziness or fainting.

Instruct patient to avoid prolonged sun exposure and to use sunscreen when going outdoors.

Category

Chemical class: Salicylanilide derivative
Therapeutic class: Anthelmintic

Pregnancy category: B

Indications

To treat beef (Taenia saginata), fish (Diphyllobothrium latum), or pork (Taenia solium) tapeworm infestations CHEWABLE
Adults. 2 g as a single dose; repeated in 7 days, if needed. Maximum: 2 g daily. Children weighing more than 34 kg (75 lb). 1.5 g as a single dose; repeated in 7 days, if needed. Maximum: 2 g daily. Children weighing 11 (24 lb) to 34 kg. 1 g as a single dose; repeated in 7 days, if needed. Maximum: 2 g daily. To treat dwarf tapeworm (Hymenolepsis nana) infestations CHEWABLE
Adults. 2 g daily for 7 days; repeated in 7 to 14 days, if needed. Children weighing more than 34 kg. 1.5 g on day 1 and then 1 g daily for next 6 days; repeated in 7 to 14 days, if needed. Maximum: 2 g daily. Children weighing 11 to 34 kg. 1 g on day 1 and then 500 mg daily for the next 6 days; repeated in 7 to 14 days, if needed. Maximum: 2 g daily.

Mechanism of Action

May alter anaerobic energy production in tapeworms by inhibiting oxidative phosphorylation in their mitochondria, which decreases synthesis of ATP. Niclosamide causes the scolex (headlike segment) and proximal segment of tapeworm to detach from intestinal wall, which leads to parasite evacuation from intestine through normal peristalsis.

Contraindications

Age under 2 years; hypersensitivity to niclosamide, other anthelmintics, or their components

Interactions

alcohol use: Decreased niclosamide effects

Side Efect

CNS: Dizziness, drowsiness, headache, light-headedness
EENT: Taste perversion
GI: Abdominal distress, anorexia, constipation, diarrhea, nausea, vomiting
SKIN: Anal pruritus, rash

Cautions

To identify infestation, collect several stool specimens before starting niclosamide therapy, as ordered, because eggs and parasite segments are released irregularly.

If patient can’t chew tablets thoroughly, crush and give them with small amount of water.

For young child, crush tablets to fine powder and mix with small amount of water to make paste.

Be aware that treatment isn’t considered successful until stools have shown no eggs or parasites for at least 3 months.

PATIENT SAFTY

Instruct patient to take niclosamide after a light meal.

For young child, instruct parent to crush tablets to fine powder and mix with small amount of water to make paste.

Urge patient to complete entire course of niclosamide therapy.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to store niclosamide in a cool, dry, dark place. Caution against storing in bathroom, near kitchen sink, or in other damp places because heat and moisture break down drug.

Inform patient that stool may need to be examined on day 7 of treatment and again 1 and 3 months after treatment.

Instruct patient to wash hands thoroughly, to wash all bedding, and to use meticulous personal and environmental hygiene to decrease the risk of autoinfection.

Caution patient against eating undercooked fish, pork, or beef.

Category

Chemical class: Pyridine alkaloid
Therapeutic class: Smoking cessation adjunct

Pregnancy category: C

(nicotine polacrilex), D (other forms of nicotine)

Indications

To relieve nicotine withdrawal symptoms, including craving CHEWING GUM
Adults. Initial: 2 or 4 mg p.r.n. or every 1 to 2 hr, adjusted to complete withdrawal by 4 to 6 mo. Maximum: 30 pieces of 2-mg gum daily or 20 pieces of 4-mg gum daily. NASAL SOLUTION
Adults. 1 to 2 sprays (1 to 2 mg) in each nostril/hr. Maximum: 5 mg/hr or 40 mg daily for up to 3 mo. ORAL INHALATION Adults and adolescents. 6 to 16 cartridges (24 to 64 mg) daily for up to 12 wk; then dosage gradually reduced over 12 wk or less. Maximum: 16 cartridges (64 mg) daily for 6 mo. TRANSDERMAL SYSTEM
Adults. Initial: 14 to 22 mg daily, adjusted to lower-dose systems over 2 to 5 mo.
DOSAGE ADJUSTMENT For adolescents and for adults weighing less than 45 kg (100 lb) and who smoke less than 10 cigarettes daily or have heart disease, initial dosage reduced to 11 to 14 mg daily and adjusted to lowerdose systems over 2 to 5 mo.

Mechanism of Action

Binds selectively to nicotinic-cholinergic receptors at autonomic ganglia, in the adrenal medulla, at neuromuscular junctions, and in the brain. By providing a lower dose of nicotine than cigarettes, this drug reduces nicotine craving and withdrawal symptoms.

Contraindications

Hypersensitivity to nicotine, its components, or components of transdermal system; life-threatening arrhythmias; nonsmokers; recovery from acute MI; severe angina pectoris; skin disorders (transdermal); temporomandibular joint disease (chewing gum)

Interactions

acetaminophen, beta blockers, imipramine, insulin, oxazepam, pentazocine,
theophylline: Possibly increased therapeutic effects of these (chewing gum,
NASAL SPRAY, transdermal system) alpha blockers, bronchodilators: Possibly increased therapeutic effects of these (chewing gum, transdermal system)
bupropion: Potentiated therapeutic effects of nicotine, possibly increased risk of hypertension sympathomimetics: Possibly decreased therapeutic effects of these (chewing gum, transdermal system) theophylline, tricyclic antidepressants: Possibly altered pharmacologic actions of these (oral inhalation) acidic beverages (citrus juices, coffee, soft drinks, tea, wine): Decreased nicotine absorption from gum if beverages consumed within 15 minutes before or while chewing gum caffeine: Increased effects of caffeine (chewing gum,
NASAL SPRAY, transdermal system)

Side Efect

CNS: Dizziness, dream disturbances, drowsiness, headache, irritability, lightheadedness, nervousness (chewing gum, transdermal system); amnesia, confusion, difficulty speaking, headache, migraine headache, paresthesia (
NASAL SPRAY); chills, fever, headache, paresthesia (oral inhalation)
CV: Arrhythmias (all forms); hypertension (chewing gum, transdermal system); peripheral edema (
NASAL SPRAY)
EENT: Increased salivation, injury to teeth or dental work, mouth injury, pharyngitis, stomatitis (chewing gum); altered taste, dry mouth (chewing gum, transdermal system); altered smell and taste, burning eyes, dry mouth, earache, epistaxis, gum disorders, hoarseness, lacrimation, mouth and tongue swelling, nasal blisters, nasal irritation or ulceration, pharyngitis, rhinitis, sinus problems, sneezing, vision changes (
NASAL SPRAY); altered taste, lacrimation, pharyngitis, rhinitis, sinusitis, stomatitis (oral inhalation)
GI: Eructation (chewing gum); abdominal pain, constipation, diarrhea, flatulence, increased appetite, indigestion, nausea, vomiting (chewing gum, transdermal system); abdominal pain, constipation, diarrhea, flatulence, hiccups, indigestion, nausea (
NASAL SPRAY); diarrhea, flatulence, hiccups, indigestion, nausea, vomiting (oral inhalation)
GU: Dysmenorrhea (chewing gum, transdermal system); menstrual irregularities (
NASAL SPRAY)
MS: Jaw and neck pain (chewing gum); arthralgia, myalgia (chewing gum, transdermal system); arthralgia, back pain, myalgia (
NASAL SPRAY); back pain (oral inhalation)
RESP: Cough (chewing gum, transdermal system); bronchitis, bronchospasm, chest tightness, cough, dyspnea, increased sputum production (
NASAL SPRAY); chest tightness, cough, dyspnea, wheezing (oral inhalation)
SKIN: Diaphoresis, erythema, pruritus, rash, urticaria (chewing gum, transdermal system); acne, flushing of face, pruritus, purpura, rash (
NASAL SPRAY); pruritus, rash, urticaria (oral inhalation)
Other: Allergic reaction (chewing gum, transdermal system); physical dependence (
NASAL SPRAY); flulike symptoms, generalized pain, withdrawal symptoms (oral inhalation)

Cautions

When administering nicotine by oral inhalation, expect optimal effect to result from continuous puffing for 20 minutes.

To avoid possible burns, remove patch before patient has an MRI.

PATIENT SAFTY

Instruct patient to read and follow package instructions to obtain best results with nicotine product.

Advise patient to notify prescriber about other she takes.

Stress that patient must stop smoking as soon as nicotine treatment starts to avoid toxicity.

For chewing gum therapy, instruct patient to wait at least 15 minutes after drinking coffee, juice, soft drink, tea, or wine. Advise her to chew gum until she detects a tingling sensation or peppery taste and then to place gum between her cheek and gum until tingling or peppery taste subsides. Then direct her to move gum to a different site until tingling or taste subsides, repeating until she no longer feels the sensation—usually about 30 minutes. Caution against swallowing the gum.

For
NASAL SPRAY, tell patient to tilt her head back and spray into a nostril. Caution against sniffing, swallowing, or inhaling spray because nicotine is absorbed through nasal mucosa.

Warn patient that prolonged use of nasal form may cause dependence.

For oral inhalation, tell patient to use 6 to 16 cartridges daily to prevent or relieve withdrawal symptoms and craving. Starting with 1 or 2 cartridges daily yields poor success. Direct patient to inhale through device like a cigarette, puffing often for 20 minutes.

For transdermal system, tell patient not to open package until just before use because nicotine is lost in the air. Advise her to apply system to clean, hairless, dry site on upper outer arm or upper body. Instruct her to change systems and rotate sites every 24 hours and not to use the same site for 7 days. To avoid possible burns, advise patient to remove patch before undergoing any MRI procedure.
WARNING Urge patient to keep all unused nicotine forms safely away from children and pets and to discard used forms carefully. (Enough nicotine may remain in used systems to poison children and pets.) Instruct her to contact a poison control center immediately if she suspects that a child has ingested nicotine.

Explain to patient with asthma or COPD that nicotine may cause bronchospasm.

Inform patient that it may take several attempts to stop smoking. Urge her to join a smoking cessation program.

Category

Chemical class: Dihydropyridine derivative
Therapeutic class: Antianginal, antihypertensive

Pregnancy category: C

Indications

To manage angina
Adults. Initial: 10 mg t.i.d., increased over 1 to 2 wk as needed. Maintenance: 10 to 20 mg t.i.d. Maximum: 180 mg daily, 30 mg/dose.
Adults. Initial: 30 to 60 mg daily, increased or decreased over 7 to 14 days based on patient response. Maximum: 90 mg daily. To manage hypertension (ADALAT CC)
Adults. Initial: 30 mg daily. Maintenance: 30 to 60 mg daily, increased or decreased over 7 to 14 days based on patient response. Maximum: 90 mg daily. (ADALAT PA)
Adults. Initial: 10 to 20 mg b.i.d., increased every 3 wk based on patient response. Maintenance: 20 mg b.i.d. Maximum: 80 mg daily. (ADALAT XL)
Adults. Initial: 30 to 60 mg daily, increased or decreased over 7 to 14 days based on patient response. Maintenance: 60 to 90 mg daily. Maximum: 120 mg daily.
Adults. 30 to 60 mg daily, increased or decreased over 7 to 14 days based on patient response. Maximum: 120 mg daily.
DOSAGE ADJUSTMENT Dosage may be reduced for elderly patients and those with heart failure or impaired hepatic or renal function. Route Onset Peak Duration P.O. (caps) 20 min Unknown Unknown

Mechanism of Action

May slow movement of calcium into myocardial and vascular smooth-muscle cells by deforming calcium channels in cell membranes, inhibiting ion-controlled gating mechanisms, and disrupting calcium release from sarcoplasmic reticulum. Decreasing intracellular calcium level inhibits smooth-muscle cell contraction and dilates arteries, which decreases myocardial oxygen demand, peripheral resistance, blood pressure, and afterload.

Contraindications

Hypersensitivity to a calcium channel blocker, secondor third-degree AV block without artificial pacemaker, sick sinus syndrome

Interactions

anesthetics (hydrocarbon inhalation): Possibly hypotension antiviral , cimetidine, dalfopristin, diltiazem, erythromycin, fluconazole, itraconazole, ketoconazole, nefazodone, other antihypertensives, prazocin, quinupristin, timolol, valproic acid, verapamil: Increased risk of hypotension benazepril: Possibly increased heart rate and hypotensive effect
beta blockers: Increased risk of profound hypotension, heart failure, and worsening of angina calcium supplements: Possibly interference with action of nifedipine carbamazepine, NSAIDs, phenobarbitone, phenytoin, rifampin, rifapentine, St. John’s wort, sympathomimetics: Possibly decreased therapeutic effects of nifedipine digoxin: Transiently increased blood digoxin level, increased risk of digitalis toxicity disopyramide, flecainide: Increased risk of bradycardia, conduction defects, and heart failure doxazocin: Decreased doxazocin effectiveness; increased nifedipine effectiveness estrogens: Possibly increased fluid retention and decreased nifedipine effects lithium: Increased risk of neurotoxicity metformin: Increased metformin absorption and plasma level tacrolimus: Decreased tacrolimus metabolism grapefruit, grapefruit juice: Possibly increased bioavailability of nifedipine high-fat meals: Possibly delayed nifedipine absorption
alcohol use: Additive hypotensive effect

Side Efect

CNS: Anxiety, ataxia, confusion, dizziness, drowsiness, headache, nervousness (possibly extreme), nightmares, paresthesia, psychiatric disturbance, syncope, tremor, weakness
CV: Arrhythmias (bradycardia, tachycardia), chest pain, heart failure, hypotension, palpitations, peripheral edema
EENT: Altered taste, blurred vision, dry mouth, epistaxis, gingival hyperplasia, nasal congestion, pharyngitis, sinusitis, tinnitus
ENDO: Gynecomastia, hyperglycemia
GI: Anorexia, constipation, diarrhea, dyspepsia, elevated liver function test results, hepatitis, nausea, vomiting
GU: Dysuria, nocturia, polyuria, sexual dysfunction, urinary frequency
HEME: Anemia, leukopenia, positive Coombs’ test, thrombocytopenia
MS: Joint stiffness, muscle cramps
RESP: Chest congestion, cough, dyspnea, respiratory tract infection, wheezing
SKIN: Dermatitis, diaphoresis, erythema multiforme, flushing, photosensitivity, pruritus, rash, urticaria

Cautions

When starting and stopping nifedipine therapy, taper it, as prescribed, over 7 to 14 days.

For closely monitored hospitalized patient with angina,dosage may be increased 10 mg every 4 to 6 hours to control chest pain.

Because of drug’s negative inotropic effect on some patients, frequently monitor heart rate and rhythm and blood pressure in patients who take a beta blocker or have heart failure or significant left ventricular dysfunction.

Monitor fluid intake and output and daily weight; fluid retention may lead to heart failure. Also assess for signs of heart failure, such as crackles, dyspnea, jugular vein distention, peripheral edema, and weight gain.

PATIENT SAFTY

Instruct patient to swallow tablets whole, not to crush, chew, or break them. Inform her that their empty shells may appear in stool.

Urge patient to take nifedipine exactly as prescribed, even when she’s feeling well. Advise her to notify prescriber if she misses two or more doses.

Urge patient not to take drug within 1 hour of a high-fat meal or grapefruit. Urge her not to alter the amount of grapefruit in her diet without consulting prescriber.
WARNING Caution patient against stopping nifedipine abruptly because angina or dangerously high blood pressure could result.

Teach patient to measure pulse rate and blood pressure, and advise her to call prescriber if they drop below accepted levels. Suggest keeping a log of weekly measurements and taking it to follow-up visits.

Instruct patient to notify prescriber immediately about chest pain, difficulty breathing, ringing in ears, and swollen gums.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Urge patient to avoid alcoholic beverages because they may worsen dizziness, drowsiness, and hypotension.

Teach patient to minimize constipation by increasing her intake of fluids, if allowed, and dietary fiber.

Emphasize the need to comply with prescribed lifestyle changes, such as alcohol moderation, low-fat or low-sodium diet, regular exercise, smoking cessation, stress reduction, and weight reduction.

Stress the need for good oral hygiene and regular dental visits.

Caution patient that hot tubs, saunas, and prolonged hot showers may cause dizziness and fainting.

Advise patient to avoid prolonged sun exposure and to wear sunscreen outdoors.

Category

Chemical class: Dihydropyridine derivative
Therapeutic class: Antihypertensive

Pregnancy category: C

Indications

To manage hypertension
Adults. 20 mg daily, increased by 10 mg every 7 days, as prescribed. Maintenance: 20 to 40 mg daily. Maximum: 60 mg daily.
DOSAGE ADJUSTMENT For patients over age 65 and patients with hepatic impairment, initial dosage reduced to 10 mg daily.

Mechanism of Action

May slow extracellular calcium movement into myocardial and vascular smoothmuscle cells by deforming calcium channels in cell membranes, inhibiting ioncontrolled gating mechanisms, and interfering with calcium release from the sarcoplasmic reticulum. By decreasing the intracellular calcium level, nisoldipine inhibits smooth-muscle cell contraction and dilates coronary and systemic arteries. As with other calcium channel blockers, these actions lead to decreased myocardial oxygen requirements and reduced peripheral resistance, blood pressure, and afterload.

Contraindications

Hypersensitivity to calcium channel blocker, secondor third-degree AV block with no artificial pacemaker, sick sinus syndrome

Interactions

beta blockers: Possibly increased risk of hypotension CYP3A4 inducers such as carbamazepine,
phenytoin: Decreased nisoldipine levels and effectiveness CYP3A4 inhibitors such as azole antifungals, cimetidine,
quinidine: Increased blood nisoldipine level; increased risk of adverse reactions
NSAIDs: Decreased antihypertensive effect of nisoldipine grapefruit, grapefruit juice: Possibly increased bioavailability of nisoldipine high-fat meals: Possibly delayed nisoldipine absorption
alcohol use: Additive hypotensive effect

Side Efect

CNS: Dizziness, headache
CV: Angina, hypotension, palpitations, peripheral edema, vasodilation
EENT: Pharyngitis, sinusitis
GI: Constipation, nausea
RESP: Bronchospasm, dyspnea
SKIN: Ras
Other: Allergic-type reaction

Cautions

Monitor pulse rate and rhythm and blood pressure before starting nisoldipine therapy, during
DOSAGE ADJUSTMENTs, and periodically throughout therapy.

Don’t break or crush tablets.

For optimal absorption, give drug 1 hour before or 2 hours after meals.

Monitor fluid intake and output and daily weight to assess for signs of fluid retention, which may lead to heart failure. Also assess for signs of heart failure, such as crackles, dyspnea, jugular vein distention, peripheral edema, and weight gain.

Monitor patient for allergic-type reaction that may include bronchospasm, especially if patient has aspirin sensitivity, because drug contains FD&C yellow no. 5 dye.

PATIENT SAFTY

Instruct patient to swallow nisoldipine tablets whole, not to break, crush, or chew them.

Advise patient to take drug 1 hour before or 2 hours after meals. Urge her not to alter amount of grapefruit products in her diet without consulting prescriber.

Urge patient to continue taking drug as prescribed, even if she feels well.
WARNING Caution patient against stopping drug abruptly because blood pressure could rise dangerously high.

Instruct patient to notify prescriber about constipation, difficulty breathing, dizziness, irregular heartbeat, nausea, severe headache, and swelling of hands or feet.

Teach patient and family how to measure blood pressure, and instruct them to notify prescriber if systolic blood pressure falls below 90 mm Hg. Suggest that patient keep a log of weekly measurements and take it to follow-up visits.

Advise patient to change positions slowly to minimize the effects of orthostatic hypotension. Inform her that hot tubs, saunas, and prolonged hot showers may worsen this adverse reaction.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Urge patient to avoid alcohol and OTC alcohol-containing without consulting prescriber. Many OTC preparations can raise blood pressure.

Emphasize the need to adhere to prescribed lifestyle changes, such as alcohol moderation, low-fat and low-sodium diet, regular exercise, smoking cessation, stress reduction, and weight reduction.

Category

Chemical class: Benzamide
Therapeutic class: Antiprotozoal

Pregnancy category: B

Indications

To treat diarrhea caused by Cryptosporidium parvum ORAL SUSPENSION, Adults and children age 12 and over. 500 mg every 12 hr with meals for 3 days. ORAL SUSPENSION Children ages 4 to 11. 200 mg (10 ml) every 12 hr with meals for 3 days. Children ages 12 months to 47 months. 100 mg (5 ml) every 12 hr with meals for 3 days. To treat diarrhea caused by Giardia lamblia ORAL SUSPENSION, Children age 12 and over.500 mg every 12 hr with meals for 3 days ORAL SUSPENSION Children ages 4 to 11. 200 mg (10 ml) every 12 hr with meals for 3 days. Children ages 12 months to 47 months. 100 mg (5 ml) every 12 hr with meals for 3 days. Route Onset Peak Duration P.O. 1–4 hr Unknown Unknown

Mechanism of Action

May destroy Cryptosporidium parvum and Giardia lamblia by interfering with enzymedependent electron transfer required for their anaerobic energy metabolism. Other unidentified mechanisms may also be involved. With loss of protozoal activity in the intestines, diarrhea ceases.

Contraindications

Hypersensitivity to nitazoxanide or its components

Interactions

other highly plasma protein–bound with narrow therapeutic indices (such as warfarin and phenytoins): Possibly increased risk of toxicity of these

Side Efect

CNS: Headache
GI: Abdominal pain, anorexia, diarrhea, nausea, vomiting

Cautions

Use nitazoxanide cautiously in children with impaired hepatic function, biliary disease, or renal insufficiency.

Prepare suspension by first tapping bottle until powder flows freely. Add 24 ml of tap water to powder and shake vigorously to suspend powder. Add another 24 ml water and shake vigorously again. Keep bottle of reconstituted suspension tightly capped.

Use oral suspension for children age 11 and under because tablets contain more nitazoxanide than is recommended for children under age 12.

PATIENT SAFTY

Tell parents of patient to give nitazoxanide with meals.

Advise parents to keep reconstituted nitazoxanide bottle tightly closed and to shake the bottle well before each use.

Instruct parents to discard any unused drug after 7 days from first opening bottle.

Inform parents of diabetic patient that oral nitazoxanide suspension contains 1.48 grams of sucrose/5 ml. Tell them that they should make sure to monitor patient’s blood glucose level closely.

Tell parents that discoloration of eyes or urine, although uncommon, may occur and is harmless.

Category

Chemical class: Nitrofuran derivative
Therapeutic class: Antibiotic

Pregnancy category: B

(except near term)

Indications

To treat acute cystitis , ORAL SUSPENSION,
Adults. 50 to 100 mg every 6 hr. Maximum: 600 mg daily or 10 mg/kg daily. Children over age 1 month. 0.75 to 1.75 mg/kg every 6 hr. Adults and children age 12 and over. 100 mg every 12 hr for 7 days. To suppress chronic cystitis , ORAL SUSPENSION,
Adults. 50 to 100 mg at bedtime. Maximum: 600 mg daily or 10 mg/kg daily. Children over age 1 month. 1 mg/kg daily at bedtime.

Mechanism of Action

Inactivates or alters bacterial ribosomal proteins and other macromolecules. This action of nitrofurantoin inhibits bacterial protein synthesis, aerobic energy metabolism, DNA synthesis, RNA synthesis, and cell wall synthesis. Nitrofurantoin is bacteriostatic at low doses and bactericidal at higher doses.

Contraindications

Age under 1 month, anuria, creatinine clearance less than 60 ml/min/1.73 m2, history of cholestatic jaundice or hepatic dysfunction with previous nitrofurantoin therapy, hypersensitivity to nitrofurantoin or parabens, oliguria, pregnancy near term

Interactions

hepatotoxic : Increased risk of hepatotoxicity magnesium trisilicate: Decreased nitrofurantoin absorption methyldopa, procainamide, hemolytics: Increased risk of toxic effects from nitrofurantoin nalidixic acid: Possibly impaired therapeutic effects of this drug neurotoxic : Increased risk of neurotoxicity probenecid, sulfinpyrazone: Increased blood nitrofurantoin level and increased risk of toxicity

Side Efect

CNS: Chills, confusion, depression, headache, neurotoxicity, peripheral neuropathy
EENT: Optic neuritis, parotitis, tooth discoloration
GI: Abdominal pain, anorexia, cholestatic jaundice, diarrhea, hepatic necrosis, hepatitis, nausea, pancreatitis, pseudomembranous colitis, vomiting
GU: Rust-colored to brown urine
HEME: Aplastic anemia, granulocytopenia, hemolytic anemia, leukopenia, megaloblastic anemia, methemoglobinemia, thrombocytopenia
MS: Arthralgia, myalgia
RESP: Asthma (in asthmatic patients), cyanosis, interstitial pneumonitis (acute), pulmonary fibrosis
SKIN: Alopecia, erythema multiforme, exfoliative dermatitis, jaundice, pruritus, rash, urticaria
Other: Anaphylaxis, angioedema, druginduced fever

Cautions

Obtain a specimen of patient’s urine for culture and sensitivity tests, as ordered; review test results if possible before giving nitrofurantoin.

Give drug with food or milk to avoid staining teeth.

Don’t crush or break capsules.

Shake oral nitrofurantoin suspension before pouring dose, and mix with food or milk, as needed.

Monitor patient for evidence of superinfection, such as abdominal pain, diarrhea, and fever. If patient develops diarrhea, it may indicate pseudomembranous colitis caused by Clostridium difficile. Notify prescriber and expect to withhold nitrofurantoin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Monitor patient for pulmonary and hepatic abnormalities because rare but severe reactions have occurred with nitrofurantoin use, especially in the elderly.

Observe patient for changes in nervous function because peripheral neuropathy, although uncommon, may become severe or irreversible. Patients with renal impairment, anemia, diabetes mellitus, electrolyte imbalance, vitamin B deficiency, or debilitating disease are at higher risk for peripheral neuropathy.

PATIENT SAFTY

Instruct patient to shake nitrofurantoin oral suspension before measuring dose and to take drug with food or milk.

Caution patient against taking any preparations that contain magnesium trisilicate during therapy.

Explain that urine may turn brown, orange, or rust-colored during therapy.

Instruct patient to complete prescribed course of therapy even if symptoms subside before course is completed.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Explain that watery or bloody stools can occur 2 or more months after nitrofurantoin therapy and can be serious, requiring prompt treatment.

Category

Chemical class: Nitrate
Therapeutic class: Antianginal, antihypertensive, vasodilator

Pregnancy category: C

Indications

To prevent or treat angina BUCCAL
Adults. 1 mg every 5 hr while awake.
Adults. 2.5, 6.5, or 9 mg every 12 hr. Frequency of doses increased to every 8 hr based on patient’s response.
Adults. 2.6 or 6.5 mg every 12 hr. Frequency of doses increased to every 8 hr based on patient’s response. S.L.
Adults. 0.3 to 0.6 mg, repeated every 5 min. Maximum: 3 tabs in 15 min or 10 mg daily. TRANSDERMAL OINTMENT
Adults. 1 to 2 (15 to 30 mg) every 8 hr. Frequency of doses increased to every 6 hr if angina occurs between doses. Maximum: 5 (75 mg)/application. TRANSDERMAL PATCH
Adults. 0.1 to 0.8 mg/hr, worn 12 to 14 hr. TRANSLINGUAL SPRAY
Adults. For treatment, 1 or 2 metered doses (0.4 or 0.8 mg) onto or under tongue, repeated every 5 min as needed. For prevention, 1 or 2 metered doses (0.4 or 0.8 mg) onto or under tongue 5 to 10 minutes before activities that could lead to acute attack. To prevent or treat angina, to manage hypertension or heart failure
IV:
Adults. 5 mcg/min, increased by 5 mcg/min every 3 to 5 min to 20 mcg/min, as prescribed, and then by 10 to 20 mcg/min every 3 to 5 min until desired effect occurs.

Mechanism of Action

May interact with nitrate receptors in vascular smooth-muscle cell membranes. This interaction reduces nitroglycerin to nitric oxide, which activates the enzyme guanylate cyclase, increasing intracellular formation of cGMP. Increased cGMP level may relax vascular smooth muscle by forcing calcium out of muscle cells, causing vasodilation. Venous dilation decreases venous return to the heart, reducing left ventricular enddiastolic pressure and pulmonary artery wedge pressure. Arterial dilation decreases systemic vascular resistance, systolic arterial pressure, and mean arterial pressure. Thus, nitroglycerin reduces preload and afterload, decreasing myocardial workload and oxygen demand. It also dilates coronary arteries, increasing blood flow to ischemic myocardial tissue. Route Onset Peak Duration P.O. * 3 min Unknown 5 hr P.O. 20–45 min Unknown 8–12 hr I.V. 1–2 min Unknown 3–5 min S.L. 1–3 min Unknown 30–60 min TransIn 30 min Unknown 4–8 hr dermal TransIn 30 min Unknown 8–24 hr dermal§ Trans2 to 4 min Unknown 30–60 min lingual

Incompatibilities

Don’t administer I.V. nitroglycerin through I.V. bags or tubing made of polyvinyl chloride. Don’t mix drug with other solutions.

Contraindications

Acute MI (S.L.), angle-closure glaucoma, cerebral hemorrhage, concurrent use of phosphodiesterase inhibitors, constrictive pericarditis (I.V.), head trauma, hypersensitivity to adhesive in transdermal form, hypersensitivity to nitrates, hypotension (I.V.), hypovolemia (I.V.), inadequate cerebral circulation (I.V.), increased intracranial pressure, orthostatic hypotension, pericardial tamponade, severe anemia

Interactions

acetylcholine, norepinephrine: Possibly decreased therapeutic effects of these heparin: Possibly decreased anticoagulant effect of heparin (I.V. nitroglycerin) opioid analgesics, other antihypertensives, vasodilators: Possibly increased orthostatic hypotension phosphodiesterase inhibitors, such as sildenafil: Possibly severe hypotensive effect of nitroglycerin sympathomimetics: Possibly decreased antianginal effect of nitroglycerin and increased risk of hypotension
alcohol use: Possibly increased orthostatic hypotension

Side Efect

CNS: Agitation, anxiety, dizziness, headache, insomnia, restlessness, syncope, weakness
CV: Arrhythmias (including tachycardia), edema, hypotension, orthostatic hypotension, palpitations
EENT: Blurred vision, burning or tingling in mouth (buccal, S.L. forms), dry mouth
GI: Abdominal pain, diarrhea, indigestion, nausea, vomiting
GU: Dysuria, impotence, urinary frequency
HEME: Methemoglobinemia
MS: Arthralgia
RESP: Bronchitis, pneumonia
SKIN: Contact dermatitis (transdermal forms), flushing of face and neck, rash

Cautions

Use nitroglycerin cautiously in elderly patients, especially those who are volume depleted or taking several medications, because of the increased risk of hypotension and falls. Hypotension may be accompanied by angina and paradoxical slowing of the heart rate. Notify prescriber if these occur, and provide appropriate treatment, as ordered.

Plan a nitroglycerin-free period of about 10 hours each day, as prescribed, to maintain therapeutic effects and avoid tolerance.

Place buccal tablets in buccal pouch with patient in sitting or lying position.

Don’t break or crush tablets or capsules. Have patient swallow them whole with a full glass of water.

Place S.L. tablet under patient’s tongue and make sure it dissolves completely.

Be sure to remove cotton from S.L. tablet container to allow quick access to drug. Buccal. Ointment. §Patch.

When applying transdermal ointment, apply correct amount on dose-measuring paper. Then place paper on hairless area of body and spread in a thin, even layer over an area at least 2 inches by 3 inches. Don’t place on cuts or irritated areas. Wash your hands after application. Rotate sites. Store at room temperature.

Open transdermal patch package immediately before use. Apply patch to hairless area, and press edges to seal. Rotate sites. Store at room temperature. If patient needs cardioversion or defibrillation, remove transdermal patch.

Don’t shake translingual spray container before administering. Have patient inhale and hold her breath, and then spray drug under or on her tongue.

Be aware that I.V. nitroglycerin should be diluted only in D5W or normal saline solution and shouldn’t be mixed with other infusions. The pharmacist should add drug to a glass bottle, not a container made of polyvinyl chloride. Don’t use a filter because plastic absorbs drug. Administer with infusion pump.

Check vital signs before every dosage adjustment and often during therapy.

Frequently monitor heart and breath sounds, level of consciousness, fluid intake and output, and pulmonary artery wedge pressure, if possible.

Store premixed containers in the dark; don’t freeze them.
WARNING Assess patient for evidence of overdose, such as confusion, diaphoresis, dyspnea, flushing, headache, hypotension, nausea, palpitations, tachycardia, vertigo, vision changes, and vomiting. Treat as prescribed by removing nitroglycerin source, if possible; elevating legs above heart level; and administering an alpha-adrenergic agonist, such as phenylephrine, as prescribed, to treat severe hypotension.

PATIENT SAFTY

Teach patient to recognize signs and symptoms of angina pectoris, including chest fullness, pain, and pressure, possibly with sweating and nausea. Pain may radiate down left arm or into neck or jaw. Inform women and those with diabetes mellitus or hypertension that they may feel only fatigue and shortness of breath.

Instruct patient to read and follow package instructions to obtain full benefits of drug.

To prevent drug tolerance, inform patient that prescriber may order a 10to 12-hour drug-free period at night (or at another time if she has chest pain at night or in the morning).

Instruct patient to swallow tablets or capsules whole—not to break, crush, or chew them—with a full glass of water.

For sublingual or buccal use, advise patient to place tablet under her tongue or in buccal pouch when angina starts and then to sit or lie down. Instruct her not to swallow drug, but to let it dissolve. Explain that moisture in her mouth helps drug absorption. If angina doesn’t subside, instruct patient to place another tablet under her tongue or in buccal pouch after 5 minutes and to repeat, if needed, for three doses total. If pain doesn’t subside after 20 minutes, urge patient to call 911 or another emergency service.

Advise patient to carry S.L. tablets in their original brown bottle in a purse or jacket pocket, but not one that will be affected by body heat. Instruct her to store drug in a dry place at room temperature and to discard cotton from container. Advise her to discard and replace S.L. tablets after 6 months.

Advise patient using transdermal ointment or patch to rotate sites to avoid skin sensitization.

Inform patient that swimming or bathing doesn’t affect transdermal forms but that hot tubs, saunas, prolonged hot showers, electric blankets, and magnetic therapy over the site may increase drug absorption and cause dizziness and hypotension.

Caution against inhaling translingual spray. Before first use, tell patient to press actuator button 10 times to prime container and then hold container upright with forefinger on top of actuator button. Tell her to open her mouth, bring container as close as possible, press actuator button firmly to release spray onto or under tongue, and release button and immediately close her mouth. Remind her to replace plastic cover on container and to not spit out the drug or rinse her mouth for 5 to 10 minutes. Tell her to reprime container by pressing actuator button twice if container hasn’t been used for more than 6 weeks. Remind patient to periodically check level of fluid in container. If it reaches the top or middle hole on side of container, more should be obtained. Caution patient not to let level of liquid get to bottom of hole.

Inform patient that nitroglycerin commonly causes headache, which typically resolves after a few days of continuous therapy. Suggest taking acetaminophen, as needed.

Advise patient to notify prescriber immediately about blurred vision, dizziness, and severe headache.

Suggest that patient change positions slowly to minimize orthostatic hypotension.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Urge patient to avoid alcohol and erectile dysfunction during therapy.

Category

Chemical class: Cyanonitrosylferrate
Therapeutic class: Antihypertensive, vasodilator

Pregnancy category: C

Indications

To treat hypertensive crisis and manage severe heart failure
IV: Adults and children. Initial: 0.25 to 0.3 mcg/kg/min, increased gradually every few minutes until blood pressure reaches desired level. Maintenance: 3 mcg/kg/min (range, 0.25 to 10 mcg/kg/min). Maximum: 10 mcg/kg/min for 10 min. Route Onset Peak Duration I.V. 1–2 min Immediate 1–10 min

Mechanism of Action

May interact with nitrate receptors in vascular smooth-muscle cell membranes. This action reduces nitroprusside to nitric oxide and then activates intracellular guanylate cyclase, which increases the cGMP level. Increased cGMP level may relax vascular smooth muscle by forcing calcium out of muscle cells. Smooth-muscle relaxation causes arteries and veins to dilate, which reduces peripheral vascular resistance and blood pressure.

Incompatibilities

Don’t mix nitroprusside with any other drug.

Contraindications

Acute heart failure with decreased peripheral vascular resistance, congenital optic atrophy, decreased cerebral perfusion, hypersensitivity to nitroprusside or its components, hypertension from aortic coarctation or AV shunting, tobacco-induced amblyopia

Interactions

dobutamine: Increased cardiac output, decreased pulmonary artery wedge pressure ganglionic blockers, general anesthetics, hypotension-producing : Increased hypotensive effect sympathomimetics: Decreased antihypertensive effect of nitroprusside

Side Efect

CNS: Anxiety, dizziness, headache, increased intracranial pressure, nervousness, restlessness
CV: Hypotension, tachycardia
ENDO: Hypothyroidism
GI: Abdominal pain, ileus, nausea, vomiting
HEME: Methemoglobinemia
MS: Muscle twitching
SKIN: Diaphoresis, flushing, rash
Other: Infusion site phlebitis

Cautions

Obtain baseline vital signs before administering nitroprusside.
WARNING Don’t give drug undiluted. Reconstitute with 2 ml D5W, and add solution to 250 to 500 ml D5W to produce 200 mcg/ml or 100 mcg/ml, respectively.

Be aware that solution is stable at room temperature for 24 hours when protected from light. Don’t use reconstituted solution if it contains particles or is blue, green, red, or darker than faint brown.

Use an infusion pump. Place opaque cover over infusion container because drug is metabolized by light. I.V. tubing doesn’t need to be covered.

Keep patient supine when starting drug or titrating dose up or down.

Monitor blood pressure continuously with intra-arterial pressure monitor. Record blood pressure every 5 minutes at start of infusion and every 15 minutes thereafter.

If patient has severe heart failure, expect to administer an inotropic drug, such as dopamine or dobutamine, as prescribed.
WARNING For patient who receives prolonged nitroprusside therapy or shortterm high-dose therapy, watch for evidence of thiocyanate toxicity (ataxia, blurred vision, delirium, dizziness, dyspnea, headache, hyperreflexia, loss of consciousness, nausea, tinnitus, vomiting). Toxicity can cause arrhythmias, metabolic acidosis, severe hypotension, and death.

Monitor serum thiocyanate level at least every 72 hours; levels above 100 mcg/ml are associated with toxicity.
WARNING Assess patient for evidence of cyanide toxicity (absence of reflexes, coma, distant heart sounds, hypotension, metabolic acidosis, mydriasis, pink skin, shallow respirations, and weak pulse). If you detect such evidence, discontinue nitroprusside, as ordered, and give 4 to 6 mg/kg sodium nitrite over 2 to 4 minutes to convert hemoglobin to methemoglobin. Follow with 150 to 200 mg/kg sodium thiosulfate. Repeat this regimen at half the original doses after 2 hours, as ordered.

PATIENT SAFTY

Advise patient to change position slowly to minimize dizziness from sudden, severe hypotension.

Category

Chemical class: Ethenediamine derivative
Therapeutic class: Antiulcer

Pregnancy category: B

Indications

To manage active duodenal ulcer Adults and adolescents. 300 mg at bedtime or 150 mg b.i.d. for 8 wk.
DOSAGE ADJUSTMENT Dosage reduced to 150 mg daily if creatinine clearance is 20 to 50 ml/min/1.73 m2; to 150 mg every other day if creatinine clearance is less than 20 ml/min/1.73 m2. To prevent recurrence of duodenal ulcer Adults and adolescents. 150 mg at bedtime.
DOSAGE ADJUSTMENT Dosage reduced to 150 mg every other day for patients with creatinine clearance of 20 to 50 ml/min/ 1.73 m2; to 150 mg every 3 days for those with creatinine clearance less than 20 ml/ min/1.73 m2. To manage acute benign gastric ulcer Adults and adolescents. 300 mg at bedtime or 150 mg b.i.d. To manage gastroesophageal reflux disease Adults and adolescents. 150 mg b.i.d. To prevent or relieve acid indigestion or heartburn Adults and adolescents. 75 mg 30 min to 1 hr before meals. Route Onset Peak Duration P.O. Unknown Unknown 10–12 hr*

Mechanism of Action

Inhibits basal and nocturnal secretion of gastric acid by reversibly and competitively blocking H2receptors, especially those in gastric parietal cells. Nizatidine also inhibits gastric acid secretion in response to stimuli, including food and caffeine.

Contraindications

Hypersensitivity to nizatidine or other H2receptor antagonists

Interactions

antacids: Decreased nizatidine bioavailability itraconazole,
ketoconazole: Decreased absorption of these salicylates: Increased blood level of these * For nocturnal acid secretion; up to 4 hr for food-stimulated acid secretion. sucralfate: Possibly decreased nizatidine absorption

Side Efect

CNS: Agitation, anxiety, confusion, depression, dizziness, fatigue, fever, hallucinations, headache, insomnia, somnolence
CV: Arrhythmias, chest pain, vasculitis
EENT: Amblyopia, dry mouth, laryngeal edema, pharyngitis, rhinitis, sinusitis
ENDO: Gynecomastia
GI: Abdominal pain, constipation, diarrhea, hepatitis, nausea, vomiting
GU: Decreased libido, hyperuricemia not associated with gout or nephrolithiasis, impotence
HEME: Anemia, aplastic anemia, eosinophilia, hemolytic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia
MS: Back pain, myalgia
RESP: Bronchospasm, cough
SKIN: Alopecia, diaphoresis, erythema multiforme, exfoliative dermatitis, jaundice, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, serum sicknesslike reaction

Cautions

Monitor CBC, BUN and serum creatinine levels, and liver function test results before and periodically during nizatidine therapy.

Don’t give within 1 hour of an antacid.

PATIENT SAFTY

Instruct patient not to take nizatidine within 1 hour of an antacid.

Urge patient to take nizatidine exactly as prescribed, even if she feels better before prescription is finished. Inform her that ulcer may take up to 8 weeks to heal.

If patient smokes, urge her to stop because smoking increases gastric acid production.

Teach patient to minimize constipation by drinking plenty of fluids (if allowed), eating high-fiber , and exercising regularly.

Instruct patient to notify prescriber immediately about abdominal pain, easy bruising, extreme fatigue, yellow skin or sclera, trouble swallowing food, bloody vomitus, or bloody or tarry stools.

Urge patient not to take nizatidine with other acid reducers.

Category

Chemical class: Catecholamine
Therapeutic class: Cardiac stimulant, vasopressor

Pregnancy category: C

Indications

To treat acute hypotension, cardiogenic shock, and septic shock
IV:
Adults. Initial: 0.5 to 1 mcg/min. Increased, as ordered, until systolic blood pressure reaches desired level. Maintenance: 2 to 12 mcg/min. Children. 0.1 mcg/kg/min. Maximum: 1 mcg/kg/min. To treat refractory shock
IV:
Adults. Up to 30 mcg/min. Route Onset Peak Duration I.V. Rapid Unknown 1–2 min

Mechanism of Action

At more than 4 mcg/min, directly stimulates alpha-adrenergic receptors and inhibits adenyl cyclase, which inhibits cAMP production. Inhibition of cAMP contricts arteries and veins and increases peripheral vascular resistance and systolic blood pressure. At less than 2 mcg/min, norepinephrine directly stimulates betaadrenergic receptors in the myocardium and increases adenyl cyclase activity, producing positive inotropic and chronotropic effects.

Contraindications

Concurrent use of hydrocarbon inhalation anesthetics, hypersensitivity to norepinephrine or its components,hypovolemia,mesenteric or peripheral vascular thrombosis

Interactions

alpha blockers: Decreased vasopressor effects of norepinephrine norepinephrine bitartrate 748
beta blockers: Decreased cardiac-stimulating effect of norepinephrine, possibly decreased therapeutic effects of both digoxin: Increased risk of arrhythmias, possibly potentiated inotropic effect doxapram: Possibly increased vasopressor effects of both ergonovine, ergotamine, methylergonovine, methysergide, oxytocin: Possibly increased vasoconstriction general anesthetics: Risk of arrhythmias guanadrel, guanethidine: Increased vasopressor response to norepinephrine, possibly severe hypertension
MAO inhibitors: Possibly life-threatening arrhythmias, hyperpyrexia, severe headache, severe hypertension, and vomiting maprotiline, tricyclic antidepressants: Possibly potentiated cardiovascular and pressor effects of norepinephrine, including arrhythmias, severe hypertension, and hyperpyrexia
methylphenidate: Possibly potentiated vasopressor effect of norepinephrine nitrates: Possibly decreased therapeutic effects of both phenoxybenzamine: Possibly arrhythmias or hypotension sympathomimetics: Increased risk of adverse cardiovascular effects thyroid hormones: Increased risk of coronary insufficiency

Side Efect

CNS: Anxiety, dizziness, headache, insomnia, nervousness, tremor, weakness
CV: Angina, bradycardia, ECG changes, edema, hypertension, hypotension, palpitations, peripheral vascular insufficiency (including gangrene), PVCs, sinus tachycardia
GI: Nausea, vomiting
GU: Decreased renal perfusion
RESP: Apnea, dyspnea
SKIN: Pallor
Other: Infusion site sloughing and tissue necrosis, metabolic acidosis

Cautions

Dilute norepinephrine concentrate for infusion in D5W, dextrose 5% in normal saline solution, or normal saline solution. Dilutions typically range from 16 to 32 mcg/ml.

Make sure solution contains no particles and isn’t discolored before administering.

Give drug with a flow-control device.

Check blood pressure every 2 to 3 minutes, preferably by direct intra-arterial monitoring, until stabilized and then every 5 minutes.
WARNING Because extravasation can cause severe tissue damage and necrosis, expect prescriber to give multiple subcutaneous injections of phentolamine (5 to 10 mg diluted in 10 to 15 ml normal saline solution) around extravasated infusion site.

If blanching occurs along vein, change infusion site and notify prescriber at once.

Monitor continuous ECG during therapy.

PATIENT SAFTY

Urge patient to immediately report burning, leaking, or tingling around I.V. site.

Category

Chemical class: Fluoroquinolone
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To treat uncomplicated UTI caused by Escherichia coli, Klebsiella pneumoniae, or Proteus mirabilis
Adults. 400 mg every 12 hr for 3 days. To treat uncomplicated UTI caused by Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Enterococcus faecalis, Proteus species, Pseudomonas aeruginosa, Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus, or Streptococcus agalactiae
Adults. 400 mg every 12 hr for 7 to 10 days. To treat complicated UTI caused by E. coli, E. faecalis, K. pneumoniae, P. aeruginosa, P. mirabilis, or Serratia marcescens
Adults. 400 mg every 12 hr for 10 to 21 days. Maximum: 800 mg daily. To treat uncomplicated gonorrhea
Adults. 800 mg as a single dose. To treat prostatitis caused by E. coli
Adults. 400 mg every 12 hr for 28 days.
DOSAGE ADJUSTMENT Dosage reduced to 400 mg daily for patients with creatinine clearance of 30 ml/min/1.73 m2or less.

Mechanism of Action

Inhibits the enzyme DNA gyrase, which unwinds and supercoils bacterial DNA before it replicates. By inhibiting this enzyme, norfloxacin interferes with bacterial cell replication and causes cell death.

Contraindications

Hypersensitivity to norfloxacin, other fluoroquinolones, or their components

Interactions

aluminum-, calcium-, or magnesiumcontaining antacids; ferrous sulfate; magnesium-containing laxatives; sucralfate; zinc: Possibly decreased absorption and blood level of norfloxacin caffeine, clozapine, ropinirole, tacrine, theophylline, tizanidine: Possibly increased blood level of these class IA antiarrhythmics, such as quinidine; class III antiarrhythmics, such as sotalol; other known to prolong QTc interval, such as disopyramide and pentamidine: Possibly prolonged QTc interval cyclosporine: Possibly increased serum creatinine and blood cyclosporine levels didanosine: Possibly decreased norfloxacin absorption glyburide: Risk of severe hypoglycemia nitrofurantoin: Possibly decreased norfloxacin effectiveness
NSAIDs: Possibly increased risk of CNS stimulation and seizures probenecid: Decreased norfloxacin excretion and risk of toxicity
warfarin: Possibly increased anticoagulant effect and risk of bleeding caffeine: Reduced clearance of caffeine leading to accumulation of caffeine in blood

Side Efect

CNS: Ataxia, confusion, dizziness, drowsiness, fever, Guillian-Barré syndrome, headache, hypoesthesia, insomnia, paresthesia, peripheral neuropathy, psychosis, seizures, tremors
CV: Prolonged QT interval, torsades de pointes, vasculitis
EENT: Decreased taste sensation, diplopia, hearing loss, stomatitis, taste perversion, tinnitus, visual changes
GI: Abdominal cramps or pain, acute hepatic necrosis or failure, diarrhea, elevated liver function test results, hepatitis, jaundice, nausea, pancreatitis, pseudomembranous colitis, vomiting
GU: Interstitial nephritis, renal failure, vaginal candidiasis
HEME: Agranulocytosis, aplastic anemia, hemolytic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia
MS: Arthralgia; myasthenia gravis exacerbation; myalgia; tendinitis; tendon inflammation, pain, or rupture
RESP: Allergic pneumonitis, dyspnea
SKIN: Blisters, diaphoresis, erythema, erythema multiforme, exfoliative dermatitis, photosensitivity, pruritus, rash, StevensJohnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, serum sickness

Cautions

Obtain urine specimen for culture and sensitivity tests before starting drug, if possible.

Determine if patient has a history of CNS disorder because drug may lower seizure threshold. Notify prescriber before starting drug, and institute seizure precautions.
WARNING Before starting therapy, determine if patient takes a class IA antiarrhythmic, such as quinidine; a class III antiarrhythmic, such as sotalol; or other that prolong the QTc interval. Also find out if patient has hypokalemia or an underlying QT-interval prolonging condition. These and conditions, especially in the elderly, may prolong the QTc interval and lead to life-threatening ventricular tachycardia or torsades de pointes in a patient taking norfloxacin.

Give drug on an empty stomach 2 hours before or after antacids, didanosine, sucralfate, or vitamins that contain iron or zinc.

Keep emergency resuscitation equipment readily available, and watch for signs of hypersensitivity, such as angioedema, dysnorfloxacin 750 pnea, jaundice, rash, and urticaria. If you suspect anaphylaxis, prepare to give epinephrine, corticosteroids, and diphenhydramine, as prescribed.

If patient has myasthenia gravis, assess her often for a change in respiratory status because drug may lead to life-threatening weakness of respiratory muscles.

Notify prescriber if patient has symptoms of peripheral neuropathy (pain, burning, tingling, numbness, weakness, or altered sensations of light touch, pain, temperature, position sense, or vibration sense), which could be permanent. Expect to stop nofloxacin.

Monitor patients prone to tendinitis, such as the elderly, athletes, and those taking corticosteroids, for complaints of tendon pain, inflammation, or rupture. If present, notify prescriber and expect to discontinue norfloxacin, place patient on bedrest with no exercise of affected limb, and obtain diagnostic tests to confirm rupture.

Monitor patient for diarrhea, which may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold norfloxacin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

PATIENT SAFTY

Instruct patient to take drug on an empty stomach with a large glass of water to prevent crystalluria. Urge her to drink several glasses of water daily during therapy.

Instruct patient to take norfloxacin at least 2 hours before or after eating, drinking milk, or taking antacids, didanosine, sucralfate, or vitamins that contain iron or zinc.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Tell patient to stop drug and report tendon pain or inflammation or abnormal changes in motor or sensory function.

Urge patient to protect skin from sunlight and to report photosensitivity at once.

Tell patient to take drug exactly as prescribed, even if symptoms subside.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and can be serious, requiring prompt treatment.

Category

Chemical class: Dibenzocycloheptene derivative
Therapeutic class: Antidepressant

Pregnancy category: D

Indications

To treat depression ,
Adults. Initial: 25 mg t.i.d. or q.i.d. Maximum: 150 mg daily. Adolescents.25 to 50 mg daily or 1 to 3 mg/kg daily in divided doses. Children ages 6 to 12. 10 to 20 mg daily or 1 to 3 mg/kg daily in divided doses.
DOSAGE ADJUSTMENT Dosage possibly reduced to 30 to 50 mg daily (in divided doses or at bedtime) for elderly patients. Route Onset Peak Duration P.O. 2–3 wk Unknown Unknown

Mechanism of Action

May interfere with reuptake of serotonin (and possibly other neurotransmitters) at presynaptic neurons, thus enhancing serotonin’s effects at postsynaptic receptors. By restoring normal neurotransmitter levels at nerve synapses, this tricyclic antidepressant may elevate mood.

Contraindications

Acute recovery phase of stroke or MI; hypersensitivity to nortriptyline, other tricyclic antidepressants, or their components; use within 14 days of MAO inhibitor therapy

Interactions

amantadine, anticholinergics, antidyskinetics, antihistamines: Possibly increased anticholinergic effects, confusion, hallucinations, nightmares; increased CNS depression anticonvulsants: Possibly increased CNS depression and risk of seizures, possibly decreased anticonvulsant effectiveness antithyroid : Possibly agranulocytosis barbiturates, carbamazepine: Possibly decreased level and effects of nortriptyline bupropion, clozapine, cyclobenzaprine, haloperidol, loxapine, maprotiline, molindone, phenothiazines,
thioxanthenes: Possibly increased sedative and anticholinergic effects, possibly increased risk of seizures cimetidine, fluoxetine: Possibly increased blood nortriptyline level and risk of toxicity
clonidine: Possibly decreased antihypertensive effect and increased CNS depression disulfiram: Possibly delirium ethchlorvynol: Possibly delirium, increased CNS depression guanadrel, guanethidine: Possibly decreased antihypertensive effect of these
MAO inhibitors: Increased risk of hypertensive crisis, severe seizures, and death oral anticoagulants: Possibly increased anticoagulant activity pimozide, probucol: Possibly arrhythmias sympathomimetics, including ophthalmic epinephrine and vasoconstrictive local anesthetics: Increased risk of arrhythmias, hyperpyrexia, hypertension, tachycardia thyroid hormones: Possibly increased therapeutic and toxic effects of both
alcohol use: Increased CNS and respiratory depression, hypertension, alcohol effects

Side Efect

CNS: Ataxia, confusion, delirium, dizziness, drowsiness, excitation, hallucinations, headache, insomnia, nervousness, nightmares, parkinsonism, stroke, suicidal ideation, tremor
CV: Arrhythmias, orthostatic hypotension
EENT: Blurred vision, dry mouth, increased intraocular pressure, taste perversion
GI: Constipation, diarrhea, heartburn, ileus, increased appetite, nausea, vomiting
GU: Sexual dysfunction, urine retention
HEME: Bone marrow depression
RESP: Wheezing
SKIN: Diaphoresis, urticaria
Other: Weight gain

Cautions

Expect to stop MAO inhibitor therapy 10 to 14 days before starting nortriptyline.

Watch patient closely (especially children, adolescents, and young adults), for suicidal tendencies, particularly when therapy starts and dosage changes because depression may worsen temporarily during these times, possibly leading to suicidal ideation.

Oral solution (10 mg/5 ml) is 4% alcohol.

Give nortriptyline with food to reduce GI reactions.

Monitor blood nortriptyline level; therapeutic range is 50 to 150 ng/ml.

Monitor ECG tracing to detect arrhythmias.

PATIENT SAFTY

Explain that oral solution contains alcohol.

Discourage alcohol consumption during therapy.

Explain that improvement may take weeks.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes and particularly if patient is a child, teenager, or young adult.

Instruct patient to change position slowly to minimize orthostatic hypotension.

Suggest that patient minimize constipation by drinking plenty of fluids (if allowed), eating high-fiber , and exercising regularly.

Category

Chemical class: Amphoteric polyene macrolide
Therapeutic class: Antifungal

Pregnancy category: Not rated

(lozenges, oral suspension, tablets, topical), A (vaginal)

Indications

To treat oropharyngeal candidiasis (thrush) LOZENGES(PASTILLES) Adults and children over age 5. 200,000 to 400,000 units dissolved in mouth 4 or 5 times daily for up to 14 days. ORAL SUSPENSION Adults and children.400,000 to 600,000 units swished and swallowed q.i.d. until at least 48 hr after symptoms subside. Infants. 200,000 units to each side of mouth q.i.d. until at least 48 hr after symptoms subside. Neonates. 100,000 units applied to each side of mouth q.i.d. until at least 48 hr after symptoms subside. Adults and adolescents. 500,000 to 1,000,000 units t.i.d. until at least 48 hr after symptoms subside. Children age 5 and over.500,000 units q.i.d. until at least 48 hr after symptoms subside. To treat cutaneous and mucocutaneous candidiasis Adults and children. 100,000 units (1 g) on affected area b.i.d. or t.i.d. for at least 2 wk. To treat vulvovaginal candidiasis VAGINAL Adults and adolescents. 100,000 units (1 tab) once or twice daily for 14 days.

Mechanism of Action

Binds to sterols in fungal cell membranes, impairing membrane integrity. Cells lose intracellular potassium and other cellular contents and, eventually, die.

Contraindications

Hypersensitivity to nystatin or its components

Side Efect

ENDO: Hyperglycemia (lozenge, oral suspension)
GI: Abdominal pain, diarrhea, nausea, vomiting (oral forms)
GU: Vaginal burning or itching (vaginal form)
SKIN: Irritation (topical forms)

Cautions

Prepare nystatin powder for oral suspension for each dose; it has no preservatives.

Gently rub nystatin cream or ointment into skin at affected area. Keep area dry and avoid occlusive dressings.

Don’t get topical form in patient’s eyes.

When treating candidal infection of feet, dust patient’s shoes, socks, and feet.

For vaginal form, use applicator supplied by manufacturer.

PATIENT SAFTY

Instruct patient to let nystatin lozenges dissolve slowly in her mouth, not to chew or swallow them.

Tell patient to swish oral suspension in her mouth as long as possible before swallowing.

Advise patient to gently rub ointment or cream into skin at affected area, to keep area dry, and to avoid occlusive dressings.

Caution patient to keep topical form away from her eyes.

Advise patient with candidal infection of feet to dust her shoes, socks, and feet with nystatin.

For vaginal form, tell patient to insert with applicator supplied by manufacturer.

Category

Chemical class: Cyclic octapeptide, somatostatin analogue
Therapeutic class: Antidiarrheal, hormone suppressant

Pregnancy category: B

Indications

To control symptoms associated with vasoactive intestinal peptide tumors (watery diarrhea) and metastatic carcinoid tumors (diarrhea and flushing)
I.M.INJECTION Adults currently receiving subcutaneous injections.20 mg every 4 wk for 2 mo, with subcutaneous doses continued for 2 to 4 wk after I.M. injections start. If patient has positive response to initial 2-mo regimen, dosage reduced to 10 mg every 4 wk. If symptoms persist or increase after initial 2-mo regimen, dosage increased to 30 mg every 4 wk, as prescribed. SUBCUTANEOUS INJECTION
Adults. Initial: 200 to 300 mcg daily in divided doses b.i.d. to q.i.d. for first 2 wk. Maintenance: Individualized. Maximum: 450 mcg daily. To treat symptoms of acromegaly, to suppress the release of growth hormone from pituitary tumors I.V.OR SUBCUTANEOUS INJECTION
Adults. Initial: 50 mcg t.i.d. Usual: 100 mcg t.i.d. Maximum: 1,500 mcg daily.
I.M.INJECTION Adults currently receiving subcutaneous injections.20 mg every 4 wk for 3 mo; then adjusted as prescribed in response to serum growth hormone level. Maximum: 40 mg every 4 wk. Route Onset Peak Duration SubQ Unknown Unknown Up to 12 hr

Mechanism of Action

Controls many types of secretory diarrhea by inhibiting secretion of serotonin and pituitary and GI hormones (including insulin, glucagon, growth hormone, thyrotropin, and, possibly, thyroid-stimulating hormone) as well as vasoactive intestinal peptides and pancreatic polypeptides (including gastrin, secretin, and motilin). Inhibiting serotonin and peptides increases intestinal absorption of water and electrolytes, decreases pancreatic and gastric acid secretions, and increases intestinal transit time by slowing gastric motility. By inhibiting hormones involved in vasodilation, octreotide increases splanchnic arterial resistance and decreases GI blood flow, hepatic vein wedge pressure, hepatic blood flow, portal vein pressure, and intravariceal pressure, thus raising seated and standing blood pressures. By inhibiting serotonin secretion, octreotide eases symptoms of acromegaly, including diarrhea, flushing, wheezing, and urinary excretion of 5-hydroxyindoleacetic acid.

Incompatibilities

Don’t mix octreotide in same syringe with fat emulsions or total parenteral nutrition solutions.

Contraindications

Hypersensitivity to octreotide or its components

Interactions

beta blockers, calcium channel blockers: Additive cardiovascular effects of these bromocriptine: Increased blood bromocriptine level cisapride: Decreased effectiveness of both cyclosporine: Decreased cyclosporine level diuretics: Increased risk of fluid and electrolyte imbalances insulin, oral antidiabetic : Increased risk of hypoglycemia quinidine, terfenadine: Decreased clearance and increased blood levels of these vitamin B12: Decreased vitamin B12 level

Side Efect

CNS: Dizziness, drowsiness, fatigue, headache, intracranial hemorrhage, migraine, paranoia, seizures, suicidal ideation
CV: Arrhythmias (including conduction abnormalities), edema, hypertension, hypotension, MI, orthostatic hypotension, Raynaud’s syndrome
EENT: Deafness, epistaxis, glaucoma, retinal vein thrombosis, sinusitis, vision changes
ENDO: Hyperglycemia, hypoglycemia, hypothyroidism, pituitary apoplexy
GI: Abdominal pain, acute cholecystitis, ascending cholangitis, biliary obstruction, cholelithiasis, cholestatic hepatitis, constipation, diarrhea, elevated liver enzymes, flatulence, gastric or peptic ulcer, GI hemorrhage, intestinal obstruction, nausea, pancreatitis, vomiting
GU: Decreased libido, hematuria, increased urine output, renal failure
HEME: Anemia, pancytopenia, thrombocytopenia
MS: Arthropathy, back pain, myalgia
RESP: Status asthmaticus, pulmonary hypertension, upper respiratory tract infection
SKIN: Alopecia, petechiae, pruritus, rash, urticaria
Other: Anaphylaxis, angioedema, dehydration, electrolyte imbalances, flulike symptoms, injection site irritation or pain

Cautions

Give octreotide by I.V. injection only in an emergency, as prescribed.

To prepare depot injection (long-acting suspension form), let powder and diluent warm to room temperature and then reconstitute according to manufacturer’s instructions. Gently inject 2 ml of supplied diluent down side of vial without disturbing depot powder. Let diluent saturate powder. After 2 to 5 minutes, check sides and bottom of vial without inverting it. Once powder is completely saturated, swirl—don’t shake—vial for 30 to 60 seconds to form suspension. Use immediately after reconstituting. octreotide acetate 754

Don’t give depot injection by subcutaneous route; give only by I.M. route and only to patients who respond to and tolerate subcutaneous drug, as prescribed.

To minimize pain, use smallest injection volume to deliver dose, and rotate injection sites.

Avoid deltoid site for I.M. use because injection site reaction and pain may result. Intragluteal injection is recommended.
WARNING To avoid worsening symptoms, expect to continue subcutaneous injections when switching to I.M. injections, as prescribed.

Be aware that octreotide increases risk of acute cholecystitis, ascending cholangitis, biliary obstruction, cholestatic hepatitis, and pancreatitis.

Monitor vital signs, bowels sounds, and stool consistency. Assess for abdominal pain and signs of gallbladder disease.

Monitor serum liver enzyme levels, as appropriate.

Monitor patient for signs of electrolyte imbalances and dehydration.

Carefully monitor diabetic patient for altered glucose control.

Monitor patient’s thyroid function, as ordered, because octreotide suppresses secretion of thyroid-stimulating hormone, which may cause hypothyroidism.

If patient has periodic symptom flare-ups, expect to give additional subcutaneous octreotide temporarily, as prescribed.

PATIENT SAFTY

Advise patient to change position slowly to minimize orthostatic hypotension.

Instruct patient to notify prescriber about

Side Efect

, especially abdominal pain, which may indicate pancreatitis.

Urge diabetic patient to check blood glucose level often.

Caution female patient of childbearing age that drug may restore fertility and, if pregnancy isn’t desired, that contraception should be used during octreotide therapy.

Category

Chemical class: Fluoroquinolone
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To treat acute, uncomplicated cystitis caused by Escherichia coli or Klebsiella pneumoniae ,
IV:
Adults. 200 mg every 12 hr for 3 days. To treat uncomplicated cystitis caused by Citrobacter diversus, Enterobacter aerogenes, Proteus mirabilis, or Pseudomonas aeruginosa ,
IV:
Adults. 200 mg every 12 hr for 7 days. To treat complicated UTI caused by C. diversus, E. coli, K. pneumoniae, P. mirabilis, or P. aeruginosa
Adults. 200 mg every 12 hr for 10 days. To treat uncomplicated gonorrhea ,
IV: Adults and adolescents. 400 mg as single dose. To treat urethritis or cervicitis caused by Chlamydia trachomatis or Neisseria gonorrhoeae ,
IV: Adults and adolescents. 300 mg b.i.d. for 7 days as an alternative to doxycycline or azithromycin. To treat pelvic inflammatory disease caused by susceptible organisms Adults and adolescents. 400 mg b.i.d. with metronidazole P.O. for 10 to 14 days.
IV: Adults and adolescents. 400 mg every 12 hr with metronidazole I.V.; then switched to oral therapy, as prescribed, after 24 hr. Full course of therapy lasts 14 days. To treat prostatitis caused by E. coli ,
IV:
Adults. 300 mg every 12 hr for 6 wk. To treat lower respiratory tract infections caused by Haemophilus influenzae or Streptococcus pneumoniae and skin and soft-tissue infections caused by Staphylococcus aureus or Streptococcus pyogenes ,
IV:
Adults. 400 mg every 12 hr for 10 days.
DOSAGE ADJUSTMENT If creatinine clearance is 20 to 50 ml/min/1.73 m2, dosing interval possibly reduced to every 24 hr; if clearance is less than 10 ml/min/1.73 m2, dosage possibly reduced by 50% and given every 24 hr.

Mechanism of Action

Inhibits synthesis of the bacterial enzyme DNA gyrase by counteracting excessive supercoiling of DNA during replication or transcription. Inhibition of DNA gyrase causes rapidand slow-growing bacterial cells to die.

Incompatibilities

Don’t mix ofloxacin with other I.V. or additives.

Contraindications

Hypersensitivity to ofloxacin, other fluoroquinolones, or their components

Interactions

aluminum-, calcium-, or magnesiumcontaining antacids; didanosine; ferrous sulfate; magnesium-containing laxatives; multivitamins; sevelamer; sucralfate; zinc: Decreased absorption of oral ofloxacin probenecid: Decreased ofloxacin excretion, increased risk of toxicity procainamide: Decreased renal clearance of procainamide
warfarin: Possibly increased anticoagulant activity and risk of bleeding

Side Efect

CNS: Aggressiveness, agitation, ataxia, dizziness, drowsiness, emotional lability, exacerbation of extrapyramidal disorders and myasthenia gravis, fever, headache, incoordination, insomnia, light-headedness, mania, peripheral neuropathy, psychotic reactions, restlessness, stroke, suicidal ideation, syncope
CV: Arrhythmias, prolonged QT interval, severe hypotension, torsades de pointes, vasculitis
EENT: Blurred vision; diplopia; disturbances in taste, smell, hearing, and equilibrium
ENDO: Hyperglycemia, hypoglycemia
GI: Abdominal cramps or pain, acute hepatic necrosis or failure, diarrhea, hepatitis, jaundice, nausea, pseudomembranous colitis, vomiting
GU: Acute renal insufficiency or failure, interstitial nephritis, renal calculi, vaginal candidiasis
HEME: Agranulocytosis, aplastic or hemolytic anemia, leukopenia, pancytopenia, thrombocytopenia
MS: Arthralgia; myalgia; rhabdomyolysis; tendinitis; tendon inflammation, pain, or rupture
RESP: Allergic pneumonitis, pulmonary edema
SKIN: Blisters, diaphoresis, erythema, erythema multiforme, exfoliative dermatitis, photosensitivity, pruritus, rash, StevensJohnson syndrome, toxic epidermal necrolysis, urticaria
Other: Acidosis, anaphylaxis, infusion site phlebitis, serum sickness

Cautions

Because of increased risk of prolonged QT interval, ofloxacin shouldn’t be used if patient has had a prolonged QT interval, has an uncorrected electrolyte disorder, or takes a Class IA or III antiarrhythmic. Monitor elderly patients closely because risk of prolonged QT interval may be increased in this group.

For I.V. infusion, dilute drug in normal saline solution or D5W to at least 4 mg/ ml, and infuse over 60 minutes to minimize the risk of hypotension. Discard unused portion.

Monitor patient closely for hypersensitivity, which may occur as early as first dose. Reaction may include angioedema, bronchospasm, dyspnea, itching, rash, jaundice, shortness of breath, and urticaria. If these signs or symptoms appear, notify prescriber immediately and expect to discontinue drug.

Notify prescriber if patient has symptoms of peripheral neuropathy (pain, burning, tingling, numbness, weakness, or altered sensations of light touch, pain, temperature, position sense, or vibration sense), which could be permanent; tendon rupture (pain and inflammation), which may occur more often in patients (especially elderly ones) taking corticosteroids and requires immediate rest; or a severe photosensitivity reaction. In each case, expect to stop ofloxacin.

Maintain adequate hydration to prevent development of highly concentrated urine and crystalluria.

Expect an increased risk of toxicity in severe hepatic disease, including cirrhosis.

Be aware that ofloxacin may stimulate the CNS and aggravate seizure disorders.

If diarrhea develops, notify prescriber because it may indicate pseudomembranous colitis. Ofloxacin may need to be discontinued and additional therapy started.

Be alert for secondary fungal infection.

PATIENT SAFTY

Encourage patient to take each oral dose with a full glass of water.

Tell patient to complete full course of ofloxacin therapy exactly as prescribed, even if he feels better before it’s complete.

Urge patient not to take antacids, iron or zinc preparations, or other (such as sucralfate and didanosine), within 2 hours of ofloxacin to prevent decreased or delayed drug absorption.

Advise patient to avoid hazardous activities until CNS effects of drug are known.

Tell patient to limit exposure to sun and ultraviolet light to prevent phototoxicity.

Advise patient to notify prescriber immediately about burning skin, hives, itching, rash, rapid heart rate, abnormal motor or sensory function, and tendon pain.

Urge patient to seek medical care immediately for trouble breathing or swallowing, which may signal an allergic reaction.

Instruct diabetic patient who takes insulin or an antidiabetic to notify prescriber immediately if he develops a hypoglycemic reaction; ofloxacin will have to be stopped.

Advise patient to notify prescriber if diarrhea develops, even up to 2 months after ofloxacin therapy ends. Additional therapy may be needed.

Category

Chemical class: Thienobenzodiazepine derivative
Therapeutic class: Antipsychotic

Pregnancy category: C

Indications

To treat psychosis ORALLY
,
Adults. Initial: 5 to 10 mg daily. Usual: 10 mg daily. Maximum: 20 mg daily. To treat manic phase of acute bipolar disorder ORALLY
,
Adults. Initial: 10 to 15 mg daily; may be increased or decreased by 5 mg every 24 hr as needed and prescribed. Usual: 5 to 20 mg daily for 3 to 4 wk. Maximum: 20 mg daily. As adjunct to treat acute bipolar disorder ORALLY
,
Adults. Initial: 10 mg daily with lithium or valproate sodium; may be increased or decreased by 5 mg every 24 hr, as needed and prescribed. Usual: 5 to 20 mg/day for 6 wk. Maximum: 20 mg daily.
DOSAGE ADJUSTMENT Initial dosage possibly reduced to 5 mg for debilitated patients, those prone to hypotension, and female nonsmokers over age 65. To treat agitation associated with schizophrenia and bipolar I mania
I.M.INJECTION
Adults. 5 to10 mg p.r.n. Repeat as needed every 2 to 4 hr.
DOSAGE ADJUSTMENT Dosage decreased to 5 mg for elderly patients and 2.5 mg for debilitated patients, those prone to hypotension, and female nonsmokers over age 65. Route Onset Peak Duration P.O. 1 wk Unknown Unknown I.M. Unknown Unknown Unknown

Mechanism of Action

May achieve antipsychotic effects by antagonizing dopamine and serotonin receptors. Anticholinergic effects may result from competitive binding to and antago-nism of the muscarinic receptors M1through M5.

Contraindications

Blood dyscrasias, bone marrow depression, cerebral arteriosclerosis, coma, coronary artery disease, hepatic dysfunction, highdose CNS depressants, hypersensitivity to olanzapine or its components, hypertension, hypotension, myeloproliferative disorders, severe CNS depression, subcortical brain damage

Interactions

anticholinergics: Increased anticholinergic effects, altered thermoregulation antihypertensives: Increased effects of both , increased risk of hypotension benzodiazepines (parenteral): Increased risk of excessive sedation and cardiorespiratory depression carbamazepine, omeprazole,
rifampin: Increased olanzapine clearance
CNS depressants: Additive CNS depression, potentiated orthostatic hypotension diazepam: Increased CNS depressant effects fluvoxamine: Decreased olanzapine clearance levodopa: Decreased levodopa efficacy lorazepam (parenteral): Possibly increased somnolence with I.M. olanzapine injection
alcohol use: Additive CNS depression, potentiated orthostatic hypotension smoking: Decreased blood olanzapine level

Side Efect

CNS: Abnormal gait, agitation, akathisia, altered thermoregulation, amnesia, anxiety, asthenia, dizziness, euphoria, fatigue, fever, headache, hypertonia, insomnia, nervousness, neuroleptic malignant syndrome, restlessness, somnolence, stuttering, suicidal ideation, tardive dyskinesia, tremor
CV: Chest pain, hyperlipidemia, hypertension, hypotension, orthostatic hypotension, peripheral edema, tachycardia
EENT: Amblyopia, dry mouth, increased salivation, pharyngitis, rhinitis
ENDO: Hyperglycemia, prolactin elevation
GI: Abdominal pain, constipation, dysphagia, hepatitis, increased appetite, nausea, thirst, vomiting
GU: Urinary incontinence, UTI
HEME: Agranulocytosis, leukopenia, neutropenia
MS: Arthralgia; back, joint, or limb pain; muscle spasms and twitching
RESP: Cough
SKIN: Ecchymosis, photosensitivity, pruritus, urticaria
Other: Anaphylaxis, angioedema, flulike symptoms, weight gain

Cautions

WARNING Olanzapine shouldn’t be used for elderly patients with dementia-related psychosis because drug increases risk of death in these patients.

Reconstitute parenteral olanzapine by dissolving contents of vial in 2.1 ml sterile water to yield 5 mg/ml. Solution should be clear yellow. Use within 1 hour.

Inject I.M. olanzapine slowly, deep into muscle mass.

Keep patient recumbent after I.M. injection of olanzapine if drowsiness, dizziness, bradycardia, or hypoventialtion occurs. Don’t let patient sit or stand up until blood pressure and heart rate have returned to baseline.

Monitor patient’s blood pressure routinely during therapy because olanzapine may cause orthostatic hypotension.

Olanzapine may worsen such conditions as angle-closure glaucoma, benign prostatic hyperplasia, and seizures.

Assess daily weight to detect fluid retention.

Notify prescriber if patient develops tardive dyskinesia or urinary incontinence.

Be alert for and immediately report signs of neuroleptic malignant syndrome.

Watch patient closely (especially children, adolescents, and young adults), for suicidal tendencies, particularly when therapy starts and dosage changes, because depression may worsen temporarily during these times, possibly leading to suicidal ideation.

Monitor patient’s lipid levels throughout therapy, as ordered, because olanzapine may cause significant elevations.

Monitor patient’s blood glucose level routinely because olanzapine may increase risk of hyperglycemia.

Monitor CBC often during first few months of therapy, especially if patient has low WBC count or history of druginduced leukopenia or neutropenia. If WBC count declines, and especially if neutrophil count drops below 1,000/mm3, expect olanzapine to be discontinued. If neutropenia is significant, also monitor patient for fever or other evidence of infection and provide appropriate treatment, as prescribed.

PATIENT SAFTY

Advise patient to avoid alcohol and smoking during olanzapine therapy.

Teach patient to open orally disintegrating tablet sachet by peeling back foil on the blister and not by pushing tablet through the foil. Immediately after opening blister, tell him to use dry hands to remove tablet and place it in his mouth. Explain that tablet will disintegrate rapidly in saliva so he can easily swallow it without liquid.

Caution patient with phenylketonuria that disintegrating olanzapine tablets contain phenylalanine.

Urge patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to change position slowly to minimize effects of orthostatic hypotension.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes and particularly if patient is a child, teenager, or young adult.

Category

Chemical class: Angiotensin II receptor antagonist
Therapeutic class: Antihypertensive

Pregnancy category: C

(first trimester), D (later trimesters)

Indications

To manage or as adjunct to manage hypertension
Adults. Initial: 20 mg daily, increased in 2 wk to 40 mg daily, if needed.
DOSAGE ADJUSTMENT Lower starting dosage is recommended for patients with possible depletion of intravascular volume, such as those treated with diuretics, especially if impaired renal function is present.

Contraindications

Hypersensitivity to olmesartan medoxomil or its components

Side Efect

CNS: Ashenia, dizziness, fatigue, headache, insomnia, vertigo
CV: Chest pain, hypercholesterolemia, hyperlipidemia, hypertriglyceridemia, peripheral edema, tachycardia
EENT: Pharyngitis, rhinitis, sinusitis
ENDO: Hyperglycemia, hyperuricemia
GI: Abdominal pain, diarrhea, gastroenteritis, indigestion, nausea, vomiting
GU: Acute renal failure, elevated BUN and serum creatinine levels, hematuria, UTI
MS: Arthralgia, arthritis, back pain, myalgia, rhabdomyolysis, skeletal pain
RESP: Bronchitis, cough, upper respiratory tract infection
SKIN: Alopecia, pruritus, rash, urticaria
Other: Angioedema, hyperkalemia, increased CK level, flulike symptoms, pain

Cautions

Expect to provide treatment such as normal saline solution I.V., as prescribed, to correct known or suspected hypovolemia before beginning olmesartan therapy.

Monitor patient for increased BUN and serum creatinine levels, especially in a patient with impaired renal function, because drug may cause acute renal failure. If increased levels are significant or persist, notify prescriber immediately.

Monitor blood pressure frequently to assess effectiveness of therapy. If blood Cell interior Angiotensin II Angiotensin II Smooth muscle cell membrane Angiotensin I ACE Cell exterior

Mechanism of Action

Olmesartan medoxomil blocks angiotensin II from binding to receptor sites in many tissues, including vascular smooth muscle and adrenal glands. Angiotensin II, a potent vasoconstrictor, is then free to stimulate the adrenal cortex to secrete aldosterone, and the inhibiting effects of angiotensin II reduce blood pressure. pressure isn’t controlled with olmesartan alone, expect to administer a diuretic, such as hydrochlorothiazide, as prescribed.
WARNING Monitor patient’s blood pressure frequently if he receives a diuretic or other antihypertensive during olmesartan therapy because of an increased risk of hypotension.

Expect to discontinue drug temporarily if patient experiences hypotension. Place patient in supine position immediately and prepare to administer normal saline solution I.V., as prescribed. Expect to resume drug therapy after blood pressure stabilizes.

If patient also receives a diuretic, provide adequate hydration, as appropriate, to help prevent hypovolemia. Watch for evidence of hypovolemia, such as hypotension with dizziness and fainting.

PATIENT SAFTY

Advise patient to avoid exercise in hot weather and excessive alcohol use to reduce the risk of dehydration and hypotension. Also instruct him to notify prescriber if he has prolonged diarrhea, nausea, or vomiting.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Explain the importance of regular exercise, proper diet, and other lifestyle changes in controlling hypertension.

Advise female patient to notify prescriber immediately about known or suspected pregnancy. Explain that if she becomes pregnant, prescriber may replace olmesartan with another antihypertensive that’s safe to use during pregnancy.

Category

Chemical class: Salicylate derivative
Therapeutic class: Bowel disease suppressant

Pregnancy category: C

Indications

To maintain remission of ulcerative colitis , Adults and adolescents. 500 mg b.i.d.

Mechanism of Action

Exerts anti-inflammatory action in GI tract after being converted by colonic bacteria to mesalamine (5-aminosalicylic acid), which inhibits cyclooxygenase. Inhibition of cyclooxygenase reduces prostaglandin production in intestinal mucosa. This in turn reduces production of arachidonic acid metabolites, which may be increased in patients with inflammatory bowel disease. Olsalazine also exerts an anti-inflammatory effect by indirectly inhibiting leukotriene synthesis, which normally catalyzes production of arachidonic acid.

Contraindications

Hypersensitivity to olsalazine, salicylates, or their components

Interactions

6-mercaptopurine, thioguanine: Increased risk of myelosuppression low-molecular-weight heparins or heparinoids: Increased risk of bleeding after neuraxial anesthesia oral anticoagulants: Possibly prolonged PT varicella vaccine: Increased risk of Reye’s syndrome

Side Efect

CNS: Anxiety, depression, dizziness, drowsiness, fatigue, fever, headache, insomnia, lethargy, paresthesia, peripheral neuropathy, vertigo
CV: Myocarditis, pericarditis, seconddegree AV block
ENDO: Hot flashes
EENT: Dry eyes and mouth, lacrimation, stomatitis, tinnitus
GI: Abdominal pain, anorexia, cholestatic jaundice, cirrhosis, diarrhea, dyspepsia, elevated liver enzymes, hepatic failure or necrosis, hepatitis, hepatotoxicity, nausea, vomiting
GU: Dysuria, hematuria, interstitial nephritis, nephrotic syndrome, urinary frequency
HEME: Aplastic or hemolytic anemia, lymphopenia, neutropenia, pancytopenia
MS: Arthralgia, joint pain, muscle spasms, myalgia
RESP: Dyspnea, interstitial lung disease
SKIN: Acne, alopecia, erythema nodosum, photosensitivity, pruritus, rash
Other: Angioedema, dehydration

Cautions

Assess patient for aspirin allergy before giving olsalazine.

If patient has severe allergies or asthma, watch closely for worsening symptoms during olsalazine therapy, and notify prescriber immediately if they occur.

Assess quantity and consistency of stools and frequency of bowel movements before, during, and after therapy.

Give drug with food to decrease adverse GI reactions.

Monitor skin for adequate hydration.

Assess patient for abdominal pain and hyperactive bowel sounds.

Monitor renal and hepatic status in patient with underlying renal or hepatic dysfunction because drug may further impair these functions.

PATIENT SAFTY

Instruct patient to take olsalazine with food.

Urge patient to continue taking drug as prescribed, even if symptoms improve.

Advise patient to watch for signs of dehydration.

Tell patient to report unusual, persistent, or severe adverse effects to prescriber.

Category

Chemical class: Recombinant IgG1K antiIgE monoclonal antibody
Therapeutic class: Antiallergenic

Pregnancy category: B

Indications

To treat moderate to severe persistent asthma in patients with positive skin test or in vitro reactivity to a perennial aeroallergen whose symptoms have been inadequately controlled with inhaled corticosteroids SUBCUTANEOUS INJECTION Adults and adolescents age 12 and over. 150 to 375 mg every 2 or 4 wk. Dose and frequency determined by body weight and blood IgE levels.
DOSAGE ADJUSTMENT Dosage adjusted for significant changes in body weight.

Mechanism of Action

Helps reduce inflammation by binding to circulating IgE and keeping it from binding to mast cells. This action inhibits degranulation and blocks release of histamine and other chemical mediators. In asthma, inflammation results when antigen reexposure causes mast cells to degranulate and release histamine and chemical mediators.

Contraindications

Hypersensitivity to omalizumab or its components

Side Efect

CNS: Dizziness, fatigue, headache, vertigo
EENT: Earache, pharyngitis, sinusitis
MS: Arm or leg pain, arthralgia, fractures
RESP: Upper respiratory tract infection
SKIN: Dermatitis, pruritus, urticaria
Other: Anaphylaxis; generalized pain; injection site bruising, burning, hive or mass formation, induration, inflammation, itching, pain, redness, stinging, and warmth; malignancies; viral infection

Cautions

Record patient’s weight, and obtain blood IgE levels, as ordered, before starting omalizumab; dosage and dosing frequency are based on these factors.

Reconstitute using sterile water for injection, and allow 15 to 20 minutes (on average) for lyophilized product to dissolve. Draw 1.4 ml sterile water for injection into a 3-ml syringe with a 1 18G needle. Place omalizumab vial upright, and inject sterile water into vial using aseptic technique. Gently swirl upright vial for about 1 minute to evenly wet powder. Don’t shake. Every 5 minutes, gently swirl for 5 to 10 seconds until solution contains no gel-like particles. Discard if powder takes longer than 40 minutes to dissolve, and start with a new vial. Once reconstituted, solution should be clear or slightly opalescent and may have a few small bubbles or foam around edge of vial. Use omalizumab within 8 hours if refrigerated or 4 hours if stored at room temperature.

To remove reconstituted omalizumab from vial, invert vial for 15 seconds to let solution drain toward stopper. Using a new 3-ml syringe with a 1 18G needle, insert needle into inverted vial and position needle tip at the very bottom of solution in the vial stopper. Then pull plunger all the way back to end of syringe barrel to remove all solution from inverted vial. To obtain full 150-mg dose (1 vial containing 1.2 ml of reconstituted omalizumab), you must withdraw all product from vial before expelling any air or excess solution from syringe.

Don’t give more than 150 mg of omalizumab per injection site.

Be prepared to inject omalizumab over 5 to 10 seconds because solution is slightly viscous.
WARNING Monitor patient closely for hypersensitivity reactions, particularly for first 2 hours after delivery. Although rare, anaphylaxis has occurred as early as first dose and more than 1 year after starting regular treatment. Keep emergency medication and equipment readily available.
WARNING Monitor patient closely for signs of cancer. Report any abnormal findings to prescriber.

PATIENT SAFTY

Instruct patient to notify prescriber immediately about possible hypersensitivity, such as rash, hives, or difficulty breathing.

Caution patient that any improvement in his asthma may take time.

Encourage patient to comply with regularly scheduled prescriber visits.

Inform patient of risk of malignancy and suggest routine cancer screening.

Explain that omalizumab isn’t used to treat acute bronchospasm or status asthmaticus.

Tell patient not to abruptly stop any prescribed systemic or inhaled corticosteroid when starting omalizumab therapy because steroid dosage must be tapered gradually under prescriber’s supervision.

If female patient becomes pregnant within 8 weeks before or during omalizumab therapy, urge her to enroll in the Xolair Pregnancy Exposure Registry at 1-866496-5247. Also, tell her to notify prescriber because drug may need to be changed.

Category

Chemical class: Ethyl esters of omega-3 fatty acids
Therapeutic class: Lipid regulator

Pregnancy category: C

Indications

As adjunct to diet to reduce triglyceride level that exceeds 500 mg/dl
Adults. 4 g once daily or 2 g b.i.d.

Mechanism of Action

Omega-3-acid ethyl esters are essential fatty acids that may inhibit very-low-density lipoprotein and triglyceride synthesis in the liver. With less triglyceride synthesis, plasma triglyceride levels decrease.

Contraindications

Hypersensitivity to omega-3-acid ethyl esters or their components

Interactions

anticogulants: Possibly increased bleeding time

Side Efect

CV: Angina pectoris
EENT: Halitosis, nosebleeds, taste perversion
GI: Diarrhea, dyspepsia, eructation, nausea, vomiting
HEME: Prolonged bleeding time
MS: Back pain
SKIN: Bruising, rash
Other: Anaphylaxis, flulike symptoms

Cautions

Be aware that known to increase triglyceride levels—such as beta blockers, thiazide diuretics, and estrogens—should be discontinued or changed, if possible, before omega-3 ethyl ester therapy starts.

Expect to check patient’s triglyceride level before starting and periodically throughout omega-3-acid ethyl ester therapy to determine effectiveness.

Administer drug with meals.

Expect to stop omega-3-acid ethyl ester therapy after 2 months if patient’s trigylceride level doesn’t decrease as expected.

PATIENT SAFTY

Explain to patient the importance of dietary measures, an exercise program, and controlling other factors—such as blood glucose level—that may contribute to elevated triclyceride levels.

Advise patient to take drug with meals.

Explain that patient will need periodic laboratory tests to evaluate therapy.

Instruct patient to seek immediate medical attention if chest pain occurs.

Category

Chemical class: Substituted benzimidazole
Therapeutic class: Antiulcer

Pregnancy category: C

Indications

To treat gastroesophageal reflux disease (GERD) without esophageal lesions, to prevent erosive esophagitis
Adults. 20 mg daily for 4 wk. To treat GERD with erosive esophagitis
Adults. 20 mg daily for 4 to 8 wk. To treat pediatric GERD and other acidrelated disorders Children age 2 and over weighing more than 20 kg. 20 mg daily. Children age 2 and over weighing 20 kg (44 lb) or less. 10 mg daily. To provide short-term treatment of active benign gastric ulcer
Adults. 40 mg daily for 4 to 8 wk.
Adults. 20 mg daily for 4 to 8 wk, increased to 40 mg daily, p.r.n. To treat duodenal or gastric ulcer associated with Helicobacter pylori
Adults. 40 mg daily with clarithromycin for 14 days, followed by 20 mg daily alone for another 14 days. Or, 20 mg b.i.d. with amoxicillin for 14 days. Or, 20 mg b.i.d. with amoxicillin and clarithromycin for 10 days.
Adults. 20 mg b.i.d. with clarithromycin and amoxicillin or metronidazole for 7 days, followed by 20 mg daily for up to 3 wk (for duodenal ulcer) or 20 to 40 mg daily for up to 12 wk (for gastric ulcer). To provide long-term treatment of gastric hypersecretory conditions, such as multiple endocrine adenoma syndrome, systemic mastocytosis, and Zollinger Ellison syndrome
Adults. 60 mg daily or in divided doses, as prescribed. Maximum: 120 mg t.i.d. Route Onset Peak Duration P.O. 1 hr In 2 hr 72–96 hr

Contraindications

Hypersensitivity to omeprazole, other proton pump inhibitors, or their components

Interactions

alprazolam, astemizole, carbamazepine, cisapride, cyclosporine, diazepam, diltiazem, erythromycin, felodipine, lidocaine, lovastatin, midazolam, quinidine, simvastatin, terfenadine, triazolam, verapamil, voriconazole: Decreased clearance and increased blood levels of these ampicillin, iron salts, itraconazole, ketoconazole, vitamin B12: Impaired absorption of these atazanavir, nelfinavir: Decreased plasma atazanavir or nelfinavir level cilostazol: Increased blood cilostazol level clarithromycin: Increased blood levels of omeprazole and clarithromycinl digoxin: Increased digoxin bioavailability, possibly digitalis toxicity levobupivacaine: Increased risk of levobupivacaine toxicity methotrexate: Possibly delayed methotrexate elimination nifedipine: Decreased nifedipine clearance, increased risk of hypotension
phenytoin: Decreased phenytoin clearance, increased risk of phenytoin toxicity saquinavir: Increased plasma saquinavir level sucralfate: Decreased omeprazole absorption tacrolimus: Possibly increased tacrolimus level
warfarin: Possibly increased risk of abnormal bleeding

Side Efect

CNS: Agitation, asthenia, dizziness, drowsiness, fatigue, headache, psychic disturbance, somnolence
CV: Chest pain, hypertension, peripheral edema
EENT: Anterior ischemic optic neuropathy, optic atrophy or neuritis, stomatitis
ENDO: Hypoglycemia
GI: Abdominal pain, constipation, diarrhea, dyspepsia, elevated liver function tests, flatulence, hepatic dysfunction or failure, indigestion, nausea, pancreatitis, vomiting
GU: Interstitial nephritis
HEME: Agranulocytosis, anemia, hemolytic anemia, leukopenia, leukocytosis, neutropenia, pancytopenia, thrombocytopenia
MS: Back pain
RESP: Cough
SKIN: Erythema multiforme, photosensitivity, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, hyponatremia

Cautions

Give omeprazole before meals, preferably in the morning for once-daily dosing. If needed, also give an antacid, as prescribed.

If needed, open capsule and sprinkle enteric-coated granules on applesauce or yogurt or mix with water or acidic fruit juice, such as apple or cranberry juice. Give immediately.

To give drug via NG tube, mix granules in acidic juice because enteric coating dissolves in alkaline pH.

Because drug can interfere with absorption of vitamin B12, monitor patient for macrocytic anemia.

Be aware that long-term use of omeprazole may increase the risk of gastric carcinoma.

PATIENT SAFTY

Tell patient to take drug before eating— usually before breakfast—and to swallow delayed-release capsules or tablets whole. If needed, patient may sprinkle contents of capsule onto 1 tablespoon of applesauce and swallow immediately without chewing pellets. Tell him to follow with a glass of cool water and not to keep any leftover mixture.

If patient takes the oral suspension, tell K+ K+ H+ H+ ClClParietal cell Blocked proton pump Omeprazole Stomach lumen Parietal cell membrane Proton pump HCl K+ K+ H+ H+ ClClParietal cell Blocked proton pump Omeprazole Stomach lumen Parietal cell membrane Proton pump HCl

Mechanism of Action

Omeprazole interferes with gastric acid secretion by inhibiting the hydrogenpotassium-adenosine triphosphatase (H+K+-ATPase) enzyme system, or proton pump, in gastric parietal cells. Normally, the proton pump uses energy from hydrolysis of adenosine triphosphate to drive hydrogen (H+) and chloride (Cl-) out of parietal cells and into the stomach lumen in exchange for potassium (K+), which leaves the stomach lumen and enters parietal cells. After this exchange, H+and Cl-combine in the stomach to form hydrochloric acid (HCl), as shown below left. Omeprazole irreversibly blocks the exchange of intracellular H+ and extracellular K+, as shown below right. By preventing H+from entering the stomach lumen, omeprazole keeps additional HCl from forming. him to empty package into a small cup containing 2 tablespoons of water (no other beverage should be used), stir the mixture well, drink it immediately, refill the cup with water, and drink again.

Encourage patient to avoid alcohol, aspirin products, ibuprofen, and that may increase gastric secretions during therapy. Tell him to notify all prescribers about prescription drug use.

Advise patient to notify prescriber immediately about abdominal pain or diarrhea.

Urge female patient of childbearing age to use effective contraception during therapy and to inform prescriber immediately if she is or suspects she may be pregnant.

Category

Chemical class: Carbazole
Therapeutic class: Antiemetic

Pregnancy category: B

Indications

To prevent chemotherapy-induced nausea and vomiting
,, Adults and children age 12 and over. Initial: 8 mg given 30 min before chemotherapy. After chemotherapy: 8 mg given 8 hr after initial dose; then 8 mg every 12 hr for 1 to 2 days. Children ages 4 to 12. Initial: 4 mg given 30 min before chemotherapy. After chemotherapy: 4 mg given 4 and 8 hr after initial dose; then 4 mg every 8 hr for 1 to 2 days.
IV:
Adults. 32 mg infused over 15 min starting 30 min before chemotherapy; or three 0.15mg/kg doses, each infused over 15 min, starting with first dose given 30 min before chemotherapy and second and third doses given 4 and 8 hours after first dose. Children ages 6 months to 18 years. Three 0.15-mg/kg doses, each infused over 15 min, starting with first dose given 30 min before chemotherapy and second and third doses given 4 and 8 hours after first dose. To prevent postoperative nausea and vomiting
,,
Adults. 16 mg as a single dose 1 hr before anesthesia induction.
I.V.INJECTION Adults and children age 12 and over. 4 mg as a single dose over 2 to 5 min just before anesthesia induction or if nausea or vomiting develops shortly after surgery. Children ages 2 to 12 weighing more than 40 kg (88 lb). 4 mg as a single dose over 2 to 5 min just before anesthesia induction or if nausea or vomiting develops shortly after surgery. Children ages 1 month to 12 years weighing less than 40 kg. 0.1 mg/kg as a single dose over 2 to 5 min just before or immediately after anesthesia induction or if nausea or vomiting develops shortly after surgery.
I.M.INJECTION Adults and children age 12 and over.4 mg as a single dose just before anesthesia induction or if nausea or vomiting develops shortly after surgery. To prevent nausea and vomiting after radiation therapy
,, Adults and children age 12 and over. Initial: 8 mg as a single dose given 1 to 2 hr before radiation therapy. Posttherapy: 8 mg every 8 hr, as needed and tolerated.
DOSAGE ADJUSTMENT For patients with hepatic impairment, maximum dosage limited to 8 mg daily I.V. or P.O.

Mechanism of Action

Blocks serotonin receptors centrally in the chemoreceptor trigger zone and peripherally at vagal nerve terminals in the intestine. This action reduces nausea and vomiting by preventing serotonin release in the small intestine (probable cause of chemotherapyand radiation-induced nausea and vomiting) and by blocking signals to the CNS. Ondansetron may also bind to other serotonin receptors and to mu-opioid receptors.

Incompatibilities

Don’t give ondansetron in same I.V. line as acyclovir, allopurinol, aminophylline, amphotericin B, ampicillin, ampicillin and sulbactam, amsacrine, cefepime, cefoperazone, furosemide, ganciclovir, lorazepam, methylprednisolone, mezlocillin, piperacillin, or sargramostim. Alkaline solutions and highly concentrated fluorouracil solutions are physically incompatible.

Contraindications

Hypersensitivity to ondansetron or its components

Interactions

cisplatin, cyclophosphamide: Possibly altered blood levels of these
alcohol use: Increased stimulant and sedative effects, including mood and physical sensations

Side Efect

CNS: Agitation, akathisia, anxiety, ataxia, dizziness, drowsiness, fever, headache, hypotension, restlessness, seizures, syncope, somnolence, weakness
CV: Arrythmias, chest pain, hypotension, pulmonary embolism, shock, tachycardia, transient prolonged QT interval
EENT: Accommodation disturbances, altered taste, blurred vision, dry mouth, laryngeal edema, laryngospasm, transient blindness
GI: Abdominal pain, anorexia, constipation, diarrhea, elevated liver function test results, flatulence, indigestion, intestinal obstruction, thirst
RESP: Bronchospasm, shortness of breath
SKIN: Flushing, hyperpigmentation, maculopapular rash, pruritus
Other: Anaphylaxis, angioedema, injection site burning, pain, and redness

Cautions

WARNING Be aware that oral disintegrating tablets may contain aspartame, which is metabolized to phenylalanine and must be used cautiously in patients with phenylketonuria.

Place disintegrating tablet on patient’s tongue immediately after opening package. It dissolves in seconds.

Use calibrated container or oral syringe to measure dose of oral solution.

Give up to 4 mg I.V. diluted in 50 ml of D5W or normal saline solution.
WARNING Be aware that ondansetron may mask symptoms of adynamic ileus or gastric distention after abdominal surgery.

PATIENT SAFTY

Advise patient to use calibrated container or oral syringe to measure oral solution.

Instruct patient to place ondansetron disintegrating tablet on his tongue immediately after opening package and to let it dissolve on his tongue before swallowing.

Advise patient to immediately report signs of hypersensitivity, such as rash.

Reassure patient with transient blindness that it will resolve within a few minutes to 48 hours.

Category

Chemical class: Lipase inhibitor
Therapeutic class: Antiobesity

Pregnancy category: B

Indications

To promote weight loss in patients with body mass index above 30 kg (66 lb)/m2 (27 kg [59.4 lb]/m2in those with diabetes mellitus, hyperlipidemia, or hypertension) and to reduce the risk of weight regain GELCAPS
Adults. 120 mg t.i.d. with fat-containing meals.

Contraindications

Cholestasis, chronic malabsorption syndrome, hypersensitivity to orlistat or its components

Interactions

cyclosporine: Altered cyclosporine absorption fat-soluble vitamins: Decreased vitamin absorption, especially vitamin E and betacarotene levothyroxine: Possibly decreased levothyroxine effectiveness, resulting in hypothyroidism pravastatin: Potentiated lipid-lowering effect

Side Efect

CNS: Anxiety, depression, dizziness, fatigue, headache, sleep disturbance
CV: Pedal edema
EENT: Gingival or tooth disorder, otitis
GI: Abdominal discomfort or pain, cholelithiasis, diarrhea (infectious), elevated liver enzyme levels, fatty or oily stool, fecal incontinence or urgency, flatulence with discharge, hepatitis, increased frequency of bowel movements, nausea, pancreatitis, rectal pain, vomiting
GU: Menstrual irregularities, UTI, vaginitis
MS: Arthralgia, arthritis, back pain, leg pain, myalgia, tendinitis
RESP: Respiratory tract infection
SKIN: Dry skin, pruritus, rash, urticaria
Other: Anaphylaxis, angioedema, flulike symptoms

Cautions

Give orlistat with or up to 1 hour after meals that contain fat.

Give levothyroxine and orlistat at least 4 hours apart because orlistat may decrease levothyroxine effectiveness, resulting in hypothyroidism.

Consult prescriber if you think patient has an eating disorder, such as anorexia nervosa or bulimia.

PATIENT SAFTY

Instruct patient to take orlistat with or shortly after meals that contain fat.

Advise patient to take a multivitamin that contains fat-soluble vitamins and betacarotene at least 2 hours before or after orlistat, if indicated.

If patient takes levothyroxine, tell him to separate it from orlistat by at least 4 hours.

Explain orlistat’s adverse GI effects and that reducing dietary fat may decrease them. Instruct him to notify prescriber if they become too unpleasant.

Help patient plan a reduced-fat diet (less than 30% of daily calories) and an exercise program to promote weight loss.

Advise patient to weigh himself daily, at the same time and wearing similar clothes, to check his progress in losing weight.

Category

Chemical class: Tertiary amine
Therapeutic class: Skeletal muscle relaxant

Pregnancy category: C

Indications

To relieve muscle spasms in painful musculoskeletal conditions (ORPHENADRINE CITRATE) Adults and adolescents. 100 mg b.i.d. in the morning and evening. (ORPHENADRINE HYDROCHLORIDE) Adults and adolescents. 50 mg t.i.d. Maximum: 250 mg daily. I.V.OR
I.M.INJECTION(ORPHENADRINE CITRATE) Adults and adolescents. 60 mg every 12 hr, p.r.n.
DOSAGE ADJUSTMENT Dosage reduced to 25 to 50 mg t.i.d. or q.i.d. if patient also receives aspirin and caffeine. Route Onset Peak Duration P.O. In 1 hr Unknown 4–6 hr* I.V. Immediate Unknown 4–6 hr I.M. 30 min Unknown 4–6 hr

Mechanism of Action

May reduce muscle spasms by acting on cerebral motor centers or medulla. Postganglionic anticholinergic effects and some antihistaminic and local anesthetic action contribute to skeletal muscle relaxation.

Contraindications

Angle-closure glaucoma; hypersensitivity to orphenadrine or its components; myasthenia gravis; obstruction of bladder neck, duodenum, or pylorus; prostatic hypertrophy; stenosing peptic ulcers

Interactions

amantadine, amitriptyline, amoxapine, antimuscarinics, atropine, bupropion, carbinoxamine, chlorpromazine, clemastine, clomipramine, clozapine, cyclobenzaprine, diphenhydramine, disopyramide, doxepin, imipramine, maprotiline, mesoridazine, methdilazine, nortriptyline, phenothiazines, procainamide, promazine, promethazine, protriptyline, thioridazine, triflupromazine, trimeprazine, trimipramine: Possibly additive anticholinergic effects
CNS depressants: Increased CNS depression
haloperidol: Increased schizophrenic symptoms, possibly tardive dyskinesia propoxyphene: Increased risk of anxiety, confusion, and tremor
alcohol use: Increased CNS depression

Side Efect

CNS: Agitation, confusion, dizziness, drowsiness, light-headedness, syncope, tremor
CV: Palpitations, tachycardia
EENT: Blurred vision, dry eyes and mouth, increased contact lens awareness
GI: Abdominal distention, constipation, nausea, vomiting
GU: Urine retention

Cautions

Be aware that orphenadrine shouldn’t be given to patients with tachycardia or cardiac insufficiency.

Give I.V. form over 5 minutes with patient in supine position. Have patient stay in this position for 5 to 10 minutes to minimize

Side Efect

. Then help him to sitting position.

Be aware that drug can aggravate myasthenia gravis and cause tachycardia.

Anticipate that drug’s anticholinergic effects may cause blurred vision, dry eyes, and increased contact lens awareness.

PATIENT SAFTY

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Explain that dry mouth may occur, and suggest increased fluid intake, ice chips, and sugarless candy or gum.

Suggest that patient (especially one who wears contact lenses) use artificial tears to avoid discomfort from dry eyes.

Category

Chemical class: Penicillin
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat bacteremia, bone and joint * 12 hr for extended-release. infections (such as osteomyelitis and infectious arthritis), CNS infections (such as ventriculitis and meningitis), endocarditis, septicemia, skin and softtissue infections, upper and lower respiratory tract infections, and UTI caused by penicillinase-producing strains of Staphylococcus or other susceptible organisms , Adults and children weighing 40 kg (88 lb) or more. 500 to 1,000 mg every 4 to 6 hr. Maximum: 6 g daily. Children weighing less than 40 kg. 50 to 100 mg/kg daily in divided doses every 4 to 6 hr. To treat mild to moderate infections caused by penicillinase-producing strains of Staphylococcus or other susceptible organisms
IV:,
I.M.INJECTION Adults and children weighing 40 kg or more.250 to 500 mg every 4 to 6 hr. Infants and children weighing less than 40 kg. 50 mg/kg daily in divided doses every 4 to 6 hr. Neonates over age 7 days weighing more than 2,000 g. 25 to 50 mg/kg every 6 hr. Neonates over age 7 days weighing less than 2,000 g. 25 to 50 mg/kg every 8 hr. Neonates age 7 days and under weighing more than 2,000 g. 25 to 50 mg/kg every 8 hr. Neonates age 7 days and under weighing 2,000 g or less. 25 to 50 mg/kg every 12 hr. To treat severe infections caused by penicillinase-producing strains of Staphylococcus or other susceptible organisms
IV:,
I.M.INJECTION Adults and children weighing 40 kg or more.1,000 mg every 4 to 6 hr. Infants and children weighing less than 40 kg. 100 to 200 mg/kg daily in divided doses every 4 to 6 hr. Neonates over age 7 days weighing more than 2,000 g. 25 to 50 mg/kg every 6 hr. Neonates over age 7 days weighing less than 2,000 g. 25 to 50 mg/kg every 8 hr. Neonates age 7 days and under weighing more than 2,000 g. 25 to 50 mg/kg every 8 hr. Neonates age 7 days and under weighing 2,000 g or less. 25 to 50 mg/kg every 12 hr. To treat endocarditis caused by methicillin-susceptible Staphylococcus aureus in patients without a prosthetic valve
IV:
Adults. 2 g every 4 hr for 4 to 6 wk. To treat endocarditis caused by methicillin-susceptible S. aureus in patients with a prosthetic valve
IV:
Adults. 2 g every 4 hr for at least 6 wk.

Mechanism of Action

Inhibits bacterial cell wall synthesis. In susceptible bacteria, the rigid, cross-linked cell wall is assembled in several steps. Oxacillin affects final stage of cross-linking process by binding with and inactivating penicillinbinding proteins (enzymes responsible for linking the cell wall strands). This action causes bacterial cell lysis and death.

Incompatibilities

Don’t give oxacillin at same time or in same admixture as aminoglycosides because they are chemically and physically incompatible and will inactivate each other.

Contraindications

Hypersensitivity to oxacillin, penicillins, or their components

Interactions

aminoglycosides: Inactivation of both chloramphenicol, erythromycins, sulfonamides, tetracyclines: Decreased therapeutic effects of oxacillin oral contraceptives: Decreased contraceptive efficacy probenecid: Increased blood oxacillin level all : Altered absorption of oxacillin

Side Efect

CNS: Anxiety, depression, fatigue, hallucinations, headache, seizures
EENT: Oral candidiasis
GI: Diarrhea, nausea, pseudomembranous colitis, vomiting
GU: Interstitial nephritis, vaginal candidiasis
HEME: Agranulocytosis, anemia, granulocytopenia, neutropenia
SKIN: Exfoliative dermatitis, pruritus, rash, urticaria
Other: Anaphylaxis

Cautions

Administer oxacillin at least 1 hour before other antibiotics.

Give oral forms on an empty stomach, preferably 1 hour before or 2 hours after a meal, to prevent impaired absorption.

Before reconstitution, tap bottle several times to loosen powder. For I.M. injection, reconstitute with sterile water for injection, half-normal (0.45) saline solution, or normal saline solution. Shake until solution is clear.

For I.V. infusion, reconstitute only with normal saline solution or D5W.

When giving drug to patient at risk for hypertension or fluid overload, be aware that each gram of oxacillin contains 4.02 mEq of sodium.

Monitor patient closely for diarrhea, which may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold oxacillin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

PATIENT SAFTY

Advise patient to take oxacillin on an empty stomach.

Instruct patient to notify prescriber immediately should a rash develop.

Advise female patient who uses an oral contraceptive to use an additional contraceptive method during oxacillin therapy.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and can be serious, requiring prompt treatment.

Category

Chemical class: Testosterone derivative
Therapeutic class: Appetite stimulant

Pregnancy category: X

Controlled susbstance schedule: III

Indications

To promote weight gain after chronic infection, extensive surgery, failure to maintain weight despite no evidence of pathology, or severe trauma; to offset protein catabolism from prolonged use of corticosteroids
Adults. 2.5 to 20 mg in divided doses given b.i.d. to q.i.d. for 2 to 4 wk; intermittent therapy repeated as prescribed. Maximum: 20 mg daily. Children. 0.1 mg/kg daily; intermittent therapy repeated as prescribed.
DOSAGE ADJUSTMENT Dosage shouldn’t exceed 5 mg b.i.d. for elderly patients.

Mechanism of Action

Promotes tissue-building processes and reverses catabolic or tissue-depleting processes by promoting protein anabolism.

Contraindications

Breast cancer (males); breast cancer with hypercalcemia (females); hypersensitivity to oxandrolone, anabolic steroids, or their components; nephrosis; pregnancy; prostate cancer

Interactions

corticosteroids: Increased risk of edema and severe acne hepatotoxic : Increased risk of hepatotoxicity insulin, oral antidiabetic : Possibly hypoglycemia NSAIDs, oral anticoagulants, salicylates: Increased anticoagulant effects sodium-containing : Increased risk of edema somatrem, somatropin: Possibly accelerated epiphyseal closure
warfarin: Increased warfarin half-life and risk of bleeding high-sodium : Increased risk of edema

Side Efect

CNS: Depression, excitement, insomnia
CV: Decreased serum HDL level, edema, hyperlipidemia, hypertension
ENDO: Feminization in postpubertal males (epididymitis, gynecomastia, impotence, oligospermia, priapism, testicular atrophy); glucose intolerance; virilism in females (acne, clitoral enlargement, decreased breast size, deepened voice, diaphoresis, emotional lability, flushing, hirsutism, hoarseness, libido changes, male-pattern baldness, menstrual irregularities, nervousness, oily skin or hair, vaginal bleeding, vaginitis, weight gain), virilism in prepubertal males (acne, decreased ejaculatory volume, penis enlargement, prepubertal closure of epiphyseal plates, unnatural growth of body and facial hair)
GI: Diarrhea, elevated liver function test results, hepatocellular carcinoma, nausea, vomiting
GU: Benign prostatic hyperplasia, prostate cancer, urinary frequency, urine retention (elderly men)
HEME: Iron deficiency anemia, leukemia, prolonged bleeding time
SKIN: Jaundice
Other: Fluid retention, hypercalcemia (females), physical and psychological dependence, sodium retention

Cautions

Use oxandrolone cautiously in patients with heart disease because drug has hypercholesterolemic effects.

Provide adequate calories and protein, as ordered, to maintain a positive nitrogen balance during oxandrolone therapy.

Anticipate an increased risk of fluid and sodium retention in patients with cardiac, hepatic, or renal dysfunction.

Weigh patient daily to detect fluid retention. If patient has fluid retention, expect a sodium-restricted diet or diuretics.
WARNING Be aware that oxandrolone may suppress spermatogenesis in males and cause permanent virilization in females.

Monitor blood glucose level frequently in patient with diabetes mellitus.

If patient takes an oral anticoagulant, check INR or PT as ordered.

PATIENT SAFTY

Advise patient to consume a diet high in protein and calories to achieve maximum therapeutic effect of oxandrolone.

Urge patient to weigh himself daily during therapy and to report swelling or unexplained weight gain at once.

Explain that drug may alter libido.

Inform woman that drug may cause permanent physical changes, such as clitoral enlargement, deepened voice, and hair growth.

Advise female patient of childbearing age that she must use contraception during oxandrolone therapy and should notify prescriber immediately about suspected or known pregnancy.

Instruct diabetic patient to monitor blood glucose level frequently.

If patient takes warfarin, advise bleeding precautions (such as an electric shaver and soft toothbrush). Tell patient to notify prescriber immediately if bleeding occurs.

Category

Chemical class: Proprionic acid derivative
Therapeutic class: Anti-inflammatory, antirheumatic

Pregnancy category: C

(first trimester), Not rated (later trimesters)

Indications

To treat rheumatoid arthritis
Adults. 1,200 mg daily. Dosage adjusted based on response. Maximum: 1,800 mg daily or 26 mg/kg daily (whichever is less) in divided doses b.i.d. or t.i.d. To treat osteoarthritis
Adults. 600 to 1,200 mg daily. Maximum: 1,800 mg daily or 26 mg/kg (whichever is less) in divided doses b.i.d. or t.i.d.
DOSAGE ADJUSTMENT Initial loading dose of 1,200 to 1,800 mg possibly given to speed onset of action. Initial dose limited to 600 mg daily for patients with renal impairment. Route Onset Peak Duration P.O. In 7 days Unknown Unknown

Mechanism of Action

Blocks cyclooxygenase, the enzyme needed to synthesize prostaglandins, which mediate the inflammatory response and cause local vasodilation, swelling, and pain. By blocking cyclooxygenase and prostaglandins, the NSAID oxaprozin relieves pain.

Contraindications

Angioedema, asthma, bronchospasm, nasal polyps, rhinitis, or urticaria induced by aspirin, iodides, or other NSAIDs

Interactions

ACE inhibitors, antihypertensives: Decreased antihypertensive response, possibly impaired renal function acetaminophen: Increased risk of adverse renal effects with long-term use of both anticoagulants, thrombolytics: Prolonged PT, increased risk of bleeding
beta blockers: Decreased antihypertensive effect bone marrow depressants: Increased risk of leukopenia and thrombocytopenia cefamandole, cefoperazone, cefotetan, plicamycin,
valproic acid: Increased risk of hypoprothrombinemia and bleeding
cimetidine: Decreased oxaprozin clearance corticosteroids, potassium supplements: Increased risk of adverse GI effects digoxin: Increased blood digoxin level and risk of digitalis toxicity diuretics: Possibly decreased diuretic effect insulin, oral antidiabetic : Increased effects of these ; risk of hypoglycemia lithium: Increased blood lithium level methotrexate: Increased blood methotrexate level and risk of methotrexate toxicity other NSAIDs, salicylates: Increased GI irritability and bleeding probenecid: Increased risk of oxaprozin toxicity alcohol use, smoking: Increased risk of adverse GI effects

Side Efect

CNS: Aseptic meningitis, cerebral hemorrhage, confusion, dizziness, drowsiness, fatigue, headache, insomnia, ischemic stroke, nervousness, sedation, transient ischemic attacks, vertigo, weakness
CV: Deep vein thrombosis, hypertension, hypotension, MI, peripheral edema
EENT: Tinnitus
ENDO: Hypoglycemia
GI: Abdominal pain, constipation, diarrhea, dyspepsia, elevated liver function test results, GI bleeding or ulceration, hepatitis, jaundice, liver failure, nausea, perforation of stomach or intestine, vomiting
GU: Acute renal failure, dysuria, interstitial nephritis, urinary frequency
HEME: Agranulocytosis, anemia, aplastic anemia, leukopenia, pancytopenia, thrombocytopenia
SKIN: Alopecia, erythema multiforme, exfoliative dermatitis, maculopapular rash, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, angioedema

Cautions

Use oxaprozin with extreme caution in patients with a history of ulcer disease or GI bleeding because NSAIDs such as oxaprozin increase risk of GI bleeding and ulceration. Expect to use oxaprozin for the shortest time possible in these patients.

Be aware that serious GI tract ulceration, bleeding, and perforation may occur without
WARNING symptoms. Elderly patients are at greater risk. To minimize risk, give drug with food. If GI distress occurs, withhold drug and notify prescriber at once.

Use oxaprozin cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.
WARNING Monitor patient closely for thrombotic events, including MI and stroke, because NSAIDs increase the risk.
WARNING If patient has bone marrow suppression or is receiving antineoplastic drug therapy, monitor laboratory results (including WBC count), and watch for evidence of infection because anti-inflammatory and antipyretic actions of oxaprozin may mask signs and symptoms, such as fever and pain.

Especially if patient is elderly or taking oxaprozin long-term, watch for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results because, in rare cases, elevated levels may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in patients with heart failure, impaired renal function, or hepatic dysfunction; those taking diuretics or ACE inhibitors; and elderly patients because drug may cause renal failure.

Monitor CBC for decreased hemoglobin level and hematocrit because drug may oxaprozin 772 worsen anemia.

Assess patient’s skin routinely for rash or other signs of hypersensitivity reaction because oxaprozin and other NSAIDs may cause serious skin reactions without warning, even in patients with no history of NSAID hypersensitivity. Stop drug at first sign of reaction, and notify prescriber.

PATIENT SAFTY

Instruct patient to take oxaprozin exactly as prescribed.

Advise patient to take drug with a full glass of water and to stay upright for 15 to 30 minutes afterward to keep drug from lodging in esophagus and causing irritation.

Urge patient to avoid alcohol as well as aspirin and other NSAIDs during oxaprozin therapy to avoid bleeding complications.

Advise patient to avoid excessive sun exposure to reduce the risk of photosensitivity.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Inform patient that risk of bleeding may continue up to 2 weeks after stopping drug.

Explain that oxaprozin may increase the risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.

Inform patient that oxaprozin also may increase the risk of serious adverse GI reactions; stress need to seek immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.

Alert patient to rare but serious skin reactions. Urge him to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity.

Category

Chemical class: Benzodiazepine
Therapeutic class: Antianxiety, sedative hypnotic

Pregnancy category: Not rated

Controlled substance schedule: IV

Indications

To treat anxiety ,
Adults. 10 to 15 mg t.i.d. or q.i.d. for mild to moderate anxiety; up to 30 mg t.i.d. or q.i.d. for severe anxiety. To help manage acute alcohol withdrawal symptoms ,
Adults. 15 to 30 mg t.i.d. or q.i.d.
DOSAGE ADJUSTMENT For elderly or debilitated patients, initial dose of 10 mg t.i.d. increased cautiously to 15 mg t.i.d. or q.i.d.

Mechanism of Action

May potentiate the effects of gammaaminobutyric acid (GABA) and other inhibitory neurotransmitters by binding to specific benzodiazepine receptors in limbic and cortical areas of the CNS. GABA inhibits excitatory stimulation, which helps control emotional behavior. The limbic system contains highly dense areas of benzodiazepine receptors, which may explain oxazepam’s antianxiety effects.

Contraindications

Acute angle-closure glaucoma; concurrent use of itraconazole or ketoconazole; hypersensitivity to oxazepam, benzodiazepines, or their components; psychoses

Interactions

cimetidine, oral contraceptives: Impaired metabolism and elimination of oxazepam clozapine: Increased risk of respiratory depression and arrest
CNS depressants: Increased risk of apnea and CNS depression levodopa: Decreased therapeutic effects of levodopa probenecid: Increased therapeutic effects of oxazepam and risk of oversedation
alcohol use: Increased risk of apnea and CNS depression

Side Efect

CNS: Anxiety (in daytime), ataxia, confusion, depression, dizziness, drowsiness, fatigue, headache, insomnia, nightmares, sleep disturbance, slurred speech, syncope, talkativeness, tremor, vertigo
GI: Nausea
Other: Drug tolerance, physical and psychological dependence, withdrawal symptoms

Cautions

WARNING Oxazepam may cause physical and psychological dependence.

Be aware that drug shouldn’t be stopped abruptly after prolonged use; doing so may cause seizures or withdrawal symptoms, such as insomnia, irritability, and nervousness.

Be aware that withdrawal symptoms can occur when therapy lasts only 1 or 2 weeks.
WARNING Monitor respiratory status in patients with pulmonary disease (such as severe COPD), respiratory depression, or sleep apnea; drug may worsen ventilatory failure.

Expect an increased risk of falls among elderly patients from impaired cognition and motor function. Take safety precautions.

Be aware that drug may worsen acute intermittent porphyria, myasthenia gravis, and severe renal impairment.

Expect patient with late-stage Parkinson’s disease to experience decreased cognition or coordination and, possibly, increased psychosis.

PATIENT SAFTY

Instruct patient to take oxazepam exactly as prescribed and not to stop taking it without consulting prescriber.

Caution patient about possible drowsiness and reduced coordination.

Urge patient to avoid alcohol, which increases oxazepam’s sedative effects.

Category

Chemical class: Tricyclic iminostilbene derivative
Therapeutic class: Anticonvulsant

Pregnancy category: C

Indications

As adjunct to treat partial seizures ORAL SUSPENSION, Adults and adolescents over age 16. Initial: 300 mg b.i.d. Dosage increased by 600 mg/ day every wk. Usual: 1,200 mg daily. Maximum: 2,400 mg daily. Children ages 4 to 16. Initial: 4 to 5 mg/kg b.i.d. to maximum initial dose of 600 mg daily. Usual: 900 mg daily for children weighing 20 to 29 kg (44 to 64 lb); 1,200 mg daily for those weighing 29.1 to 39 kg (65 to 86 lb); 1,800 mg daily for those weighing more than 39 kg. Maximum: 1,800 mg daily.
DOSAGE ADJUSTMENT For patients with creatinine clearance less than 30 ml/min/ 1.73 m2, usual initial dosage reduced by 50%. As monotherapy to treat partial seizures ORAL SUSPENSION, Adults and adolescents over age 16. Initial: 300 mg b.i.d. Dosage increased by 300 mg/ day every 3 days as needed. Usual: 1,200 mg daily. Maximum: 2,400 mg daily. Children ages 4 to 16. Initial: 4 to 5 mg/kg b.i.d., increased by 5 mg/kg daily every third day to maximum maintenance dosage, as needed. Maximum: 900 mg daily for children weighing 20 to 24.9 kg (44 to 55 lb); 1,200 mg daily for those weighing 25 to 34.9 kg (55 to 77 lb); 1,500 mg daily for those weighing 35 to 49.9 kg (77 to 110 lb); 1,800 mg daily for those weighing 50 to 59.9 kg (110 to 132 lb); 2,100 mg daily for those weighing 60 to 70 kg (132 to 154 lb). To convert to monotherapy in treating partial seizures ORAL SUSPENSION, Adults and adolescents over age 16. Initial: 300 mg b.i.d. Dosage increased by 600 mg daily every wk over 2 to 4 wk, as needed, while dosage of other anticonvulsant is reduced. Usual: 1,200 mg daily. Maximum: 2,400 mg daily. Children ages 4 to 16. Initial: 4 to 5 mg/kg b.i.d., increased by 10 mg/kg daily weekly as needed to maximum maintenance dosage while dosage of other anticonvulsant is reduced over 3 to 6 wk. Maximum: 900 mg daily for children weighing 20 to 24.9 kg (44 to 55 lb); 1,200 mg daily for those weighing 25 to 34.9 kg (55 to 77 lb); 1,500 mg daily for those weighing 35 to 49.9 kg (77 to 110 lb); 1,800 mg daily for those weighing 50 to 59.9 kg (110 to 132 lb); 2,100 mg daily for those weighing 60 to 70 kg (132 to 154 lb).

Mechanism of Action

May prevent or halt seizures by closing or blocking sodium channels in neuronal cell membrane. By preventing sodium from entering the cell, oxcarbazepine may slow nerve impulse transmission, thus decreasing the rate at which neurons fire.

Contraindications

Hypersensitivity to carbamazepine, oxcarbazepine, or their components

Interactions

carbamazepine, phenobarbital, phenytoin,
valproic acid: Decreased blood oxcarbazepine level, possibly increased blood levels of phenobarbital and phenytoin felodipine, verapamil: Decreased blood levels of these oral contraceptives: Decreased effectiveness
alcohol use: Possibly additive CNS depressant effects

Side Efect

CNS: Abnormal gait, ataxia, dizziness, fatigue, fever, headache, somnolence, suicidal ideation, tremor
EENT: Abnormal vision, diplopia, nystagmus, rhinitis
GI: Abdominal pain, indigestion, nausea, vomiting
SKIN: Rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylalxis, hyponatremia

Cautions

Patient with allergic reaction to carbamazepine may have hypersensitivity to oxcarbazepine.

Monitor serum sodium level for signs of hyponatremia, especially during first 3 months.

Monitor therapeutic oxcarbazepine levels during initiation and titration, and expect to adjust dosage accordingly.

Implement seizure precautions as needed.

Monitor patient’s skin closely. If a reaction develops, notify prescriber at once because skin reactions caused by oxcarbazepine may be serious or life-threatening.
WARNING Watch closely for evidence of multi-organ hypersensitivity, such as fever, rash, organ dysfunction, lymphadenopathy, hepatitis, liver function abnormalities, hematologic abnormalities, pruritus, nephritis, oliguria, hepato-renal syndrome, arthralgia, and asthenia. If suspected, notify prescriber and expect to stop drug. Provide supportive care, as prescribed.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

PATIENT SAFTY

Teach patient to shake suspension well and prepare dose immediately afterward. Tell him to then withdraw prescribed amount using supplied oral dosing syringe. Instruct him to mix dose in a small glass of water just before taking it, or tell him that he can swallow drug directly from syringe. Instruct him to close bottle and rinse syringe with warm water and let it dry thoroughly.

Inform patient that he may experience dizziness, double vision, and unsteady gait.

Instruct patient not to drink alcohol during oxcarbazepine therapy.

Alert patient to possibility of hypersensitivity or serious skin reactions and need to report them to prescriber.

Warn patient to notify prescriber immediately if he develops a fever; rash; swelling of face, eyes, lips, tongue; difficulty swallowing or breathing; or other evidence of hypersensitivity because drug may need to be stopped and emergency medical care given.

Alert woman of childbearing age that oxcarbazepine may render hormonal contraceptives ineffective. Urge patient to use an additional or a different contraceptive during oxcarbazepine therapy.

Urge caregivers to watch patient closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes, and to report concerns to prescriber at once.

Category

Chemical class: Xanthine derivative
Therapeutic class: Bronchodilator

Pregnancy category: C

Indications

To treat acute asthma, bronchospasm due to chronic bronchitis or COPD DELAYED-RELEASE Adults and children age 6 and over.300 mg daily for 3 days; then increased to 400 mg daily for 3 days. Maintenance: 600 mg daily in divided doses every 6 to 8 hr. Adults and children age 6 and over.300 mg daily for 3 days; then increased to 400 mg daily for 3 days. Maintenance: 600 mg daily in divided doses every 12 hr.

Mechanism of Action

Inhibits phosphodiesterase enzymes, causing bronchodilation. Normally, these enzymes inactivate cAMP and cGMP, which are responsible for bronchial smoothmuscle relaxation. Other mechanisms of action may include calcium translocation, prostaglandin antagonism, catecholamine stimulation, inhibition of cGMP metabolism, and adenosine receptor antagonism.

Contraindications

Hypersensitivity to oxtriphylline, xanthines, or their components; peptic ulcer; seizure disorder unless controlled by an anticonvulsant

Interactions

activated charcoal, aminoglutethimide, barbiturates, ketoconazole, rifampin, sulfinpyrazone, sympathomimetics: Decreased blood theophylline level allopurinol, beta blockers (nonselective), calcium channel blockers, cimetidine, corticosteroids, disulfiram, ephedrine, influenza virus vaccine, interferon, macrolides, mexiletine, oral contraceptives, quinolones, thiabendazole: Increased blood theophylline level benzodiazepines, propofol: Possibly antagonized sedative effects of these carbamazepine, isoniazid, loop diuretics: Possibly altered blood theophylline level halothane anesthetics: Increased risk of cardiotoxicity hydantoins: Possibly decreased blood hydantoin level ketamine: Increased risk of seizures lithium: Decreased blood lithium level neuromuscular blockers: Possibly reversal of neuromuscular blockade tetracyclines: Possibly increased adverse effects of theophylline all : Altered bioavailability and absorption of oxtriphylline charcoal broiled beef; low-carbohydrate, highprotein diet: Increased theophylline elimination high-carbohydrate, low-protein diet: Decreased elimination and prolonged halflife of theophylline
alcohol use: Increased CNS effects, especially with elixir smoking (1 or more packs daily): Decreased effects of oxtriphylline

Side Efect

CNS: Anxiety, dizziness, headache, insomnia, restlessness, seizures
CV: Hypotension, palpitations, sinus tachycardia
EENT: Unpleasant taste
GI: Anorexia, diarrhea, nausea, vomiting
RESP: Tachypnea
SKIN: Alopecia, flushing, rash

Cautions

Be aware that oxtriphylline contains 64% anhydrous theophylline, so dosage is based on equivalent of 5 to 6 mg of anhydrous theophylline/kg.

Be aware that food delays absorption of delayed-release and forms and that large volumes of fluid may increase absorption.

Know that delayed-release and preparations vary in their absorption rate.

Monitor blood theophylline level because toxicity may develop at a level only slightly above therapeutic.

PATIENT SAFTY

If patient complains of GI discomfort, suggest taking drug with or just after meals.

Urge patient to stop smoking and to notify prescriber about changes in smoking habits. Also instruct him to avoid alcohol during oxtriphylline therapy.

Encourage patient to keep follow-up appointments for laboratory studies.

Category

Chemical class: Tertiary amine
Therapeutic class: Antispasmodic

Pregnancy category: B

Indications

To treat overactive bladder, including neurogenic bladder, with urinary frequency, urgency, or incontinence from involuntary contraction of detrusor muscle
Adults. Initial: 5 mg daily, adjusted by 5 mg/ wk, as prescribed. Maximum: 30 mg daily. SYRUP,
Adults. 5 mg b.i.d. or t.i.d. Maximum: 5 mg q.i.d. or 20 mg daily. Children age 5 and over. 5 mg b.i.d. Maximum: 15 mg t.i.d. TRANSDERMAL SYSTEM
Adults. System supplying 3.9 mg daily, applied twice weekly. TOPICAL GEL
Adults. 1 sachet (containing 100 mg/g oxybutynin chloride gel) applied once daily to dry, intact skin on the abdomen, upper arms, shoulders, or thighs.
DOSAGE ADJUSTMENT For elderly patients, possibly 2.5 mg b.i.d. initially, increased to maximum of 5 mg t.i.d., as prescribed. Route Onset Peak Duration P.O. 30–60 min 3–6 hr 6–10 hr TransUnknown 24–48 hr 96 hr dermal

Mechanism of Action

Exerts antimuscarinic (atropine-like) and potent direct antispasmodic (papaverinelike) actions on smooth muscle in the bladder and decreases detrusor muscle contractions. The result is increased bladder capacity and a decreased urge to void.

Contraindications

Acute hemorrhage, angle-closure glaucoma, gastric retention (gel form), GI obstruction, hypersensitivity to oxybutynin or its components, ileus, intestinal atony in elderly or debilitated patients, myasthenia gravis, obstructive uropathy, toxic megacolon with ulcerative colitis, urine retention (gel form)

Interactions

amantadine, amitriptyline, amoxapine, antimuscarinics, brompheniramine, bupropion, carbinoxamine, chlorpheniramine, chlorpromazine, clemastine, clomipramine, clozapine, cyclobenzaprine, dimenhydrinate, diphenhydramine, disopyramide, doxepin, doxylamine, imipramine, maprotiline, mesoridazine, methdilazine, nortriptyline, procainamide, promazine, promethazine, protriptyline, thioridazine, triflupromazine, trimeprazine, trimipramine: Increased anticholinergic effects
CNS depressants: Increased sedation
ketoconazole: Possibly altered total absorption rate and blood level of ketoconazole opioid agonists: Increased depressive effects on GI motility and bladder function parasympathomimetics: Decreased antimuscarinic action of oxybutynin
alcohol use: Increased sedation

Side Efect

CNS: Agitation, asthenia, confusion, dizziness, drowsiness, fatigue, hallucinations, headache, insomnia, memory impairment, nervousness, psychosis, restlessness, seizures, somnolence
CV: Arrhythmias, hypertension, hypotension, palpitations, peripheral edema, QTinterval prolongation, tachycardia, vasodilation
EENT: Blurred vision; cycloplegia; dry eyes, mouth, nose, and throat; keratoconjunctivitis sicca; eye irritation; mydriasis; nasopharyngitis; rhinitis; sinusitis
ENDO: Hyperglycemia, suppression of lactation
GI: Abdominal pain, constipation, decreased GI motility, diarrhea, dysphagia, esophagitis, flatulence, gastroesophageal reflux, indigestion, nausea, vomiting
GU: Cystitis, dysuria, impotence, urinary hesitancy, urine retention, UTI
MS: Arthralgia, arthritis, back pain
RESP: Asthma, bronchitis, cough, upper respiratory tract infection
SKIN: Decreased sweating, dry skin, flushing, pruritus, rash, urticaria
Other: Application site reactions (anesthesia, dermatitis, erythema, irritation, papules, pruritus), flulike symptoms, fungal infections, heatstroke

Cautions

Use oxybutynin cautiously in patients with diarrhea because it may signal incomplete GI obstruction, especially in patients with colostomy or ileostomy. Also use cautiously in patients with dementia because drug may aggravate symptoms.

Use cautiously in patients with myasthenia gravis or GI disorders because drug may adversely affect these conditions.

Assess urinary symptoms before and after treatment.

Make sure patient swallows tablets whole and doesn’t crush, chew, or divide them. Expect to see portions of drug in stool.

Apply transdermal system to dry, intact skin of abdomen, hip, or buttock; avoid using same site for at least 7 days by rotating sites.

Apply gel form to dry, intact skin on patient’s abdomen, upper arms, shoulders, or thighs. Rotate application sites.
WARNING Watch for adverse cardiovascular reactions in patients with arrhythmias, coronary artery disease, heart failure, or hypertension because drug’s antimuscarinic effects may increase their risk.

Decreased GI motility can cause adynamic ileus; assess for abdominal pain and ileus.

Be aware that drug may aggravate benign prostatic hyperplasia, gastroesophageal reflux disease, and hyperthyroidism.

Monitor patient for anticholinergic CNS effects, such as hallucinations, agitation, confusion and somnolence, especially in the first few months of therapy or when dosage is increased. If such effects occur, notify prescriber and expect dosage to be reduced or drug discontinued.

PATIENT SAFTY

Instruct patient to take oxybutynin on an empty stomach. If adverse GI reactions develop, suggest taking drug with food or milk.

Advise patient to swallow tablets whole and not to chew, crush, or break them.

Instruct patient how to apply transdermal system or gel. Tell her to apply to clean, dry skin, avoiding areas that have been recently shaved or have open sores or rashes. Remind patient to wash hands after handling product.

Warn patient that gel is flammable and that she should avoid open fire or smoking until gel has dried. Also tell patient to avoid bathing, swimming, showering, exercising, or immersing application site in water for 1 hour after application and to cover site with clothing once gel has dried.

Warn of possible decreased alertness, and advise patient against performing hazardous activities until drug’s CNS effects are known.

Caution patient to avoid strenuous exercise and excessive sun exposure because of increased risk of heatstroke.

Urge patient to avoid alcohol during therapy.

Category

Chemical class: Phenanthrene derivative
Therapeutic class: Analgesic

Pregnancy category: Not rated

Controlled substance schedule: II

Indications

To relieve moderate to severe pain

ORALL

Adults. 5 mg every 3 to 6 hr, p.r.n., and increased as needed.
Adults. 5 mg every 3 to 6 hr or 10 mg every 6 to 8 hr, p.r.n. To manage pain for more than a few days , Adults who haven’t received opioids before. Initial: 10 to 20 mg every 12 hr, adjusted every 1 to 2 days, as prescribed, based on total amount of oxycodone needed daily to control pain. Adults who currently receive an opioid agonist or fixed-ratio combination (opioid agonist plus acetaminophen, aspirin,or NSAID). Half the 24-hr oxycodone dose every 12 hr, as prescribed. Be prepared to manage breakthrough pain with immediate-release tablets, p.r.n., and adjust every 1 to 2 days, as prescribed. Adults who use fentanyl transdermal patch. 10 mg oxycodone for each 25 mcg/ hr of fentanyl patch dosage every 12 hr, beginning 12 to 18 hr after removing patch.
DOSAGE ADJUSTMENT To provide supplemental analgesia for adults receiving controlled-release oxycodone, one-fourth to one-third the 12-hr controlled-release dose given as tablet every 3 to 6 hr, p.r.n. Route Onset Peak Duration P.O. 10–15 min 1 hr 3–4 hr

Mechanism of Action

Alters perception of and emotional response to pain at spinal cord and higher levels of CNS by blocking release of inhibitory neurotransmitters, such as gamma-aminobutyric acid and acetylcholine.

Contraindications

Hypercapnia, hypersensitivity to oxycodone or its components, ileus, use within 14 days of MAO inhibitor therapy

Interactions

anticholinergics: Possibly severe constipation and ileus antidiarrheals: Possibly severe constipation and additive CNS depression antihypertensives: Possibly exaggerated antihypertensive effects and risk of orthostatic hypotension butorphanol, pentazocine: Possibly acute withdrawal symptoms in opioid-dependent patients, decreased analgesic effects carbamazepine, phenytoin, primidone, rifampin: Possibly need for increased oxycodone dosage to achieve analgesia and prevent withdrawal symptoms in opioid-dependent patients
cimetidine: Possibly apnea, confusion, disorientation, and seizures from respiratory depression and impaired CNS function
CNS depressants: Possibly increased CNS and respiratory depression and orthostatic hypotension
MAO inhibitors: Possibly fatal reactions, including cardiac arrest, coma, respiratory depression, seizures, and severe hypertension nalbuphine, nalmefene, naloxone,
naltrexone: Blocked oxycodone effects, withdrawal symptoms in opioid-dependent patients
alcohol use: Additive CNS effects

Side Efect

CNS: Abnormal dreams, anxiety, asthenia, chills, dizziness, drowsiness, euphoria, excitation, headache, insomnia, nervousness, sedation, seizures, somnolence, syncope, twitching
CV: Bradycardia, chest pain, hypotension, orthostatic hypotension, palpitations
EENT: Blurred vision, dry eyes or mouth, lens opacities, miosis
ENDO: Syndrome of inappropriate antidiuretic hormone secretion
GI: Abdominal pain, anorexia, constipation, diarrhea, dyspepsia, elevated liver function test results, gastritis, hiccups, nausea, vomiting
GU: Amenorrhea, decreased libido, erectile dysfunction, oliguria, urinary hesitancy, urine retention
RESP: Dyspnea, respiratory depression
SKIN: Diaphoresis, pruritus, rash
Other: Anaphylaxis, drug tolerance, hyponatremia, physical and psychological dependence, withdrawal symptoms

Cautions

WARNING Be aware that oxycodone has a high potential for abuse.
WARNING Be aware that abuse of crushed controlled-release tablets poses a hazard of overdose and death. If you suspect abuse and determine that patient also is abusing alcohol or illicit substances, notify prescriber immediately because risk of overdose and death is increased. If you suspect parenteral abuse, be aware that tablet excipients, especially talc, may result in local tissue necrosis, infection, pulmonary granulomas, endocarditis, and valvular heart injury.

Assess baseline neurologic status before each dose in patient with head injury because oxycodone may obscure progression of his condition.

Assess patient’s pain level regularly, and give drug as prescribed before pain becomes severe.

Be prepared to adjust dosage for patient who hasn’t previously received opioids until he can tolerate drug’s effects.

Expect to give controlled-release tablets only to opioid-tolerant patients who need at least 160 mg daily.

Assess patient for possible respiratory depression or paradoxical excitation during dosage titration.

Assess patient for abdominal pain because oxycodone may mask underlying GI disorders.

PATIENT SAFTY

WARNING Strongly warn patient to swallow oxycodone tablets whole and not to break, chew, or crush them because taking broken, chewed, or crushed tablets leads to rapid release and absorption of a potentially fatal dose.

Instruct patient not to take oxycodone more often than prescribed and not to stop abruptly after long-term use.

Instruct patient to avoid alcohol and hazardous activities during therapy.

Tell patient to notify prescriber about signs of possible toxicity or hypersensitivity, such as excessive light-headedness, extreme dizziness, itching, swelling, and trouble breathing.

Category

Chemical class: Testosterone derivative
Therapeutic class: Antianemic, antiangioedema (hereditary)

Pregnancy category: X

Controlled substance schedule: III

Indications

To treat acquired and congenital aplastic anemias, anemias caused by deficient RBC production, bone marrow failure anemias, hypoplastic anemias caused by myelotoxic , and myelofibrosis; to prevent or treat hereditary angioedema Adults and children.1 to 2 mg/kg daily for 3 to 6 mo. Maximum: 5 mg/kg daily.

Mechanism of Action

Combats anemia by increasing production of erythropoietin, a precursor of RBCs. Oxymetholone also increases hemoglobin level and RBC volume.

Contraindications

Breast or prostate cancer in men, hypercalcemia in women with breast cancer, hypersensitivity to oxymetholone or anabolic steroids, nephrosis, nephrotic phase of neph-ritis, pregnancy, severe hepatic dysfunction

Interactions

corticosteroids: Increased risk of edema and severe acne hepatotoxic : Increased risk of hepatotoxicity insulin, oral antidiabetic : Possibly hypoglycemia NSAIDs, oral anticoagulants, salicylates: Increased anticoagulant effects sodium-containing : Increased risk of edema somatrem, somatropin: Possibly accelerated epiphyseal maturation high-sodium : Increased risk of edema

Side Efect

CNS: Depression, excitement, insomnia
CV: Decreased serum HDL level, edema, hyperlipidemia, hypertension
ENDO: Feminization in postpubertal males (epididymitis, gynecomastia, impotence, oligospermia, priapism, testicular atrophy), glucose intolerance, virilism in females (acne, clitoral enlargement, decreased breast size, deepened voice, diaphoresis, emotional lability, flushing, hirsutism, hoarseness, libido changes, male-pattern baldness, menstrual irregularities, nervousness, oily hair or skin, vaginal bleeding, vaginitis, weight gain), virilism in prepubertal males (acne, decreased ejaculatory volume, penis enlargement, prepubertal closure of epiphyseal plates, unnatural growth of body and facial hair)
GI: Diarrhea, elevated liver function test results, hepatocellular carcinoma, nausea, vomiting
GU: Benign prostatic hyperplasia, prostate cancer, urinary frequency, urine retention (elderly men)
HEME: Iron deficiency anemia, leukemia, prolonged bleeding time
SKIN: Jaundice
Other: Fluid retention, hypercalcemia (females), physical and psychological dependence, sodium retention

Cautions

Be aware that oxymetholone shouldn’t be used in patients with a history of hypercalcemia because drug may exacerbate this condition or in patients with prostate problems because drug may promote benign or cancerous tumor growth.

Anticipate increased risk of fluid and sodium retention in patients with cardiac, hepatic, or renal dysfunction. Monitor for signs and symptoms of fluid retention.

Monitor daily weight. Expect to place patient with fluid retention on sodiumrestricted diet or diuretics, as prescribed.
WARNING Be aware that oxymetholone may suppress spermatogenesis in males and cause permanent virilization in females.

PATIENT SAFTY

Advise patient to consume a diet high in protein and calories to achieve maximum therapeutic effect of oxymetholone.

Instruct patient to check his weight daily during oxymetholone therapy and to notify prescriber immediately about swelling or unexplained weight gain.

Inform patient that drug may alter libido.

Advise diabetic patient to monitor blood glucose levels frequently because drug may increase hypoglycemic effect of antidiabetic .

Inform female patient that drug may cause permanent physical changes, such as clitoral enlargement, deepened voice, and unnatural hair growth.

Advise female patient of childbearing age to use contraception during therapy and to notify prescriber immediately about suspected or known pregnancy.

Category

Chemical class: Phenanthrene derivative
Therapeutic class: Analgesic

Pregnancy category: Not rated

Controlled substance schedule: II

Indications

To relieve moderate to severe pain
Adults. Initial: 5 to 20 mg every 4 to 6 hr, p.r.n. To relieve moderate to severe pain in patients requiring continuous, aroundthe-clock opioid treatment for an extended time
Adults. Initial: 5 mg every 12 hr, increased as needed in 5to 10-mg increments every 3 to 7 days.
DOSAGE ADJUSTMENT For patients with creatinine clearance less than 50 ml/min/ 1.73 m2or elderly patients, dosage started at lowest level and titrated slowly. For patients receiving other CNS depressants, dosage started at one-third to one-half the usual starting dose. To relieve moderate to severe pain, to relieve anxiety in patients with dyspnea from pulmonary edema caused by acute left ventricular dysfunction
I.V.INJECTION
Adults. Initial: 0.5 mg, repeated every 3 to 6 hr, p.r.n. I.M.OR SUBCUTANEOUS INJECTION
Adults. Initial: 1 to 1.5 mg, repeated every 3 to 6 hr, p.r.n. SUPPOSITORIES
Adults. 5 mg every 4 to 6 hr, p.r.n. To relieve obstetric pain during labor
I.M.INJECTION
Adults. 0.5 to 1 mg as a single dose.

Mechanism of Action

Alters perception of and emotional response to pain at spinal cord and higher levels of CNS by blocking release of inhibitory neurotransmitters, such as gamma-aminobutyric acid and acetylcholine.

Contraindications

Acute or severe asthma; hypercarbia; hypersensitivity to oxymorphone, other morphine analogues, or their components; ileus; moderate to severe hepatic impairment; pulmonary edema from a chemical respiratory irritant; severe respiratory depression; upper airway obstruction Route Onset Peak Duration I.V. 5–10 min 15–30 min 3–4 hr I.M. 10–15 min 30–90 min 3–6 hr SubQ 10–20 min 30–90 min 3–6 hr P.R. 15–30 min 2 hr 3–6 hr

Interactions

anticholingerics: Increased risk of urine retention, severe constipation antidiarrheals, antiperistaltics: Increased risk of severe constipation, CNS depression antihypertensives, diuretics, hypotensionproducing : Increased hypotensive effects buprenorphine: Reduced oxymorphone effectiveness if buprenorphine is given first, possibly withdrawal symptoms in oxymorphone-dependent patients
CNS depressants: Additive CNS depressant effects, increased risk of habituation hydroxyzine, other opioid analgesics: Increased analgesia, CNS depression, and hypotensive effects
MAO inhibitors: Increased risk of unpredictable, severe, sometimes fatal

Side Efect

metoclopramide: Antagonized effects of metoclopramide on GI motility naloxone: Antagonized analgesic, CNS, and respiratory depressant effects of oxymorphone
naltrexone: Withdrawal symptoms in oxymorphone-dependent patients neuromuscular blockers: Additive respiratory depression
alcohol use: Additive CNS depressant effects, increased risk of habituation

Side Efect

CNS: Agitation, asthenia, CNS depression, confusion, delusions, depersonalization, dizziness, drowsiness, euphoria, fatigue, hallucinations, headache, insomnia, lightheadedness, nervousness, nightmares, restlessness, seizures, somnolence, tiredness, tremor, weakness
CV: Bradycardia, hypertension, hypotension, palpitations, tachycardia
EENT: Blurred vision, diplopia, dry mouth, laryngeal edema, laryngospasm, miosis, tinnitus
GI: Abdominal cramps or pain, anorexia, bilary colic, constipation, hepatotoxicity, ileus, nausea, vomiting
GU: Decreased urine output, dysuria, urinary frequency and hesitancy, urine retention
MS: Muscle rigidity (with large doses), uncontrolled muscle movements
RESP: Apnea, atelectasis, bradypnea, bronchospasm, dyspnea, irregular breathing, respiratory depression, wheezing
SKIN: Dermatitis, diaphoresis, erythema, flushing of face, pruritus, urticaria
Other: Angioedema, injection site burning, pain, redness, and swelling

Cautions

Use with extreme caution in patients with increased intracranial pressure or head injury because oxymorphone may obscure neurologic signs of increasing severity.

Use cautiously in patients with mild hepatic impairment because drug is metabolized in liver; impaired renal function because drug is excreted by kidneys; and biliary tract disease because drug may cause spasm of sphincter of Oddi.

Use cautiously in patients receiving mixed agonist-antagonist opioid analgesics because these may reduce analgesic effect of oxymorphone or may cause withdrawal symptoms.

Use cautiously in elderly patients because plasma oxymorphone levels are higher in elderly than in younger patients.

Oral hydromorphone shouldn’t be used “as needed”or for first 24 hours after surgery in patients not already taking opioids because of the risk of oversedation and respiratory depression.

If patient is being converted from one form of drug to another, watch closely for analgesic effectiveness and adverse reactions. For conversion from immediaterelease oral form to extended-release oral form, expect to give half the total daily oxymorphone hydrochloride 782 dose every 12 hours. For conversion from parenteral to oral oxymorphone, expect that you may give 10 times the total daily parenteral dose as tablets, divided into equal doses and given over 24 hours.

Taper dosage, as ordered, before stopping therapy to prevent withdrawal in physically dependent patients.

Monitor vital signs during oxymorphone therapy to detect respiratory depression and hypotension, especially in elderly patients, debilitated patients, and those with conditions accompanied by hypoxia, when even moderate doses may severely decrease pulmonary ventilation.

Monitor urinary and bowel status; constipation may be so severe it causes ileus.

Offer fluids to relieve dry mouth.

PATIENT SAFTY

Instruct patient to take oxymorphone exactly as prescribed and not to stop abruptly; warn that drug can cause physical dependence.

Stress importance of taking drug before pain becomes severe.

Instruct patient prescribed tablet form to take it on an empty stomach.

Tell patient prescribed extended-release tablet form not to break, chew, dissolve, or crush tablets before taking them because going so will lead to a rapid drug release and increased risk of a potentially fatal dose.

Instruct patient to store suppositories in refrigerator.

Encourage patient to increase fluid and fiber intake during therapy to prevent constipation.

Stress need to avoid alcohol and CNS depressants during therapy because of risk of severe life-threatening adverse reactions.

Caution patient to avoid potentially hazardous activities until drug’s CNS effects are known.

Advise female patient to stop drug and notify prescriber about known or suspected pregnancy.

Category

Chemical class: Tetracycline derived from Streptomyces rimosus
Therapeutic class: Antibiotic, antiprotozoal

Pregnancy category: D

Indications

To treat systemic bacterial and protozoal infections, such as bronchitis, chlamydial infection, Lyme disease, nongonococcal urethritis, rickettsial infection, traveler’s diarrhea, and UTI (OXYTETRACYCLINE HYDROCHLORIDE) Adults and adolescents. 250 to 500 mg every 6 hr. Maximum: 4,000 mg daily. Children ages 8 to 12. 6.25 to 12.5 mg/kg every 6 hr.
I.M.INJECTION(OXYTETRACYCLINE) Adults and adolescents. 100 mg every 8 hr, 150 mg every 12 hr, or 250 mg daily. Maximum: 500 mg daily. Children ages 8 to 12. 5 to 8.3 mg/kg every 8 hr or 7.5 to 12.5 mg/kg every 12 hr. Maximum: 250 mg daily.
DOSAGE ADJUSTMENT Dosage possibly reduced for patients with renal impairment. To treat brucellosis (OXYTETRACYCLINE HYDROCHLORIDE) Adults and adolescents. 500 mg every 6 hr for 3 wk with 1,000 mg of streptomycin I.M. every 12 hr in wk 1 and daily in wk 2. Maximum: 4,000 mg daily. To treat uncomplicated gonorrhea (OXYTETRACYCLINE HYDROCHLORIDE) Adults and adolescents. Initial: 1,500 mg, then 500 mg every 6 hr to total of 9,000 mg for full course of treatment. To treat syphilis (OXYTETRACYCLINE HYDROCHLORIDE) Adults and adolescents. 500 to 1,000 mg every 6 hr for 10 to 15 days to total of 30 to 40 g for full course of treatment.

Mechanism of Action

Binds with ribosomal subunits of susceptible bacteria and alters cytoplasmic membrane, inhibiting bacterial protein synthesis and rendering the organism ineffective.

Contraindications

Hypersensitivity to tetracyclines or their components

Interactions

antacids, calcium supplements, cholestyramine, choline salicylates, colestipol, iron supplements, magnesium salicylates: Possibly decreased absorption of oxytetracycline digoxin: Increased blood digoxin level lithium: Altered blood lithium level
methoxyflurane: Increased risk of nephrotoxicity oral anticoagulants: Increased anticoagulant effects oral contraceptives: Decreased contraceptive effectiveness, increased risk of breakthrough bleeding and pregnancy penicillins: Decreased bactericidal effects of penicillins sodium bicarbonate: Possibly decreased absorption of oral oxytetracycline vitamin A: Increased risk of benign intracranial hypertension all , especially dairy products: Possibly interference with oxytetracycline absorption

Side Efect

CNS: Dizziness, light-headedness, tiredness, unsteadiness, weakness
EENT: Darkened, discolored, or sore tongue; stomatitis, tooth discoloration (in infants and children under age 8)
GI: Abdominal cramps, diarrhea, indigestion, nausea, thirst, vomiting
GU: Urinary frequency
SKIN: Photosensitivity
Other: Superinfection

Cautions

WARNING Be aware that oxytetracycline shouldn’t be given to premature infants because it may impair skeletal growth or to children under age 8 because it may permanently discolor teeth and cause enamel hypoplasia.

For an adult, give I.M. injection in upper outer quadrant of buttocks or mid-lateral thigh; deltoid muscle may be used but only if well developed. In children, give injection only in mid-lateral thigh.

Be aware that patient should be switched from parenteral to oral form as soon as possible.

PATIENT SAFTY

Instruct patient to take oxytetracycline capsules 1 hour before meals and 3 hours before or after other and dairy products.

Advise patient to take drug with a full glass of water and in an upright position to minimize adverse GI reactions.

Urge patient to complete entire course of oxytetracycline therapy, even if he feels better beforehand.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to avoid excessive sun exposure and to protect skin when outdoors.

Urge female patient who uses oral contraceptives to use an additional form of birth control during oxytetracycline therapy.

Advise patient to discard outdated capsules because drug may become toxic.

Category

Chemical class: Benzisoxazole derivative
Therapeutic class: Antipsychotic (Atypical)

Pregnancy category: C

Indications

To treat schizophrenia
Adults. Initial: 6 mg once daily in the morning; then increased or decreased in increments of 3 mg daily every 6 or more days, as needed. Maximum: 12 mg daily.
DOSAGE ADJUSTMENT For patients with mild renal impairment (creatinine clearance 50 to 79 ml/min/1.73 m2), maximum dosage is 6 mg daily. For patients with moderate to severe renal impairment (creatinine clearance less than 50 ml/min/ 1.73 m2), maximum dosage is 3 mg daily. Route Onset Peak Duration P.O. Unknown 24 hr Unknown

Mechanism of Action

The main active metabolite of risperidone, paliperidone selectively blocks serotonin and dopamine receptors in mesocortical tract of CNS to suppress psychotic symptoms.

Contraindications

AV block, cardiac arrhythmias, congenital heart disease, history of congenital long-QT syndrome; hypersensitivity to paliperidone, risperidone, or its components

Interactions

antiarrhythmics of class IA (such as quinidine, procainamide) and class III (such as amiodarone, sotalol), antibiotics (such as gatifloxacin, moxifloxacin), antipsychotics (such as chlorpromazine, thioridazine): Increased risk of QT-interval prolongation antihypertensives: Increased antihypertensive effects bromocriptine, levodopa, pergolide: Possibly antagonized effects of these carbamazepine: Decreased paliperidone level
CNS depressants: Additive CNS depression paroxetine: Possible increased blood paliperidone level
alcohol use: CNS depression

Side Efect

CNS: Agitation, akathisia, anxiety, asthenia, dizziness, dyskinesia, dystonia, extrapyramidal disorder, fatigue, fever, headache, hyperkinesia, hypertonia, neuroleptic malignant syndrome, parkinsonism, somnolence, syncope, tardive dyskinesia, tremor
CV: Bundle branch block, first-degree heart block, hypertension, orthostatic hypotension, palpitations, prolonged QT interval, tachycardia, venous thrombosis
EENT: Blurred vision, dry mouth, salivary hypersecretion, swollen tongue
ENDO: Hyperglycemia
GI: Dyspepsia,nausea,upper abdominal pain
GU: Priapism
HEME: Agranulocytosis, leukopenia, neutropenia, thrombocytopenia
MS: Back or limb pain
RESP: Cough, dyspnea
Other: Anaphylaxis, weight gain

Cautions

Paliperidone shouldn’t be used to treat dementia-related psychosis in the elderly because of an increased mortality risk.

Drug shouldn’t be given if patient has a condition that severely narrows GI tract because tablet doesn’t change shape as it passes and could cause blockage.
WARNING Immediately notify prescriber and expect to stop drug if patient shows signs of neuroleptic malignant syndrome (altered mental status, autonomic instability, hyperpyrexia, muscle rigidity).

Monitor patient for involuntary, dyskinetic movements. Notify prescriber if present, and expect to stop therapy. In some cases, therapy may need to continue despite tardive dyskinesia.

Monitor blood glucose level because drug increases risk of hyperglycemia and possible ketoacidosis or hyperosmolar coma.

DOSAGE ADJUSTMENTs of paliperidone may be needed when carbamazepine therapy is started or discontinued because of carbamazepine’s interaction with paliperidone. P P

Check CBC often during first few months of therapy, especially if patient has low WBC count or history of drug-induced leukopenia or neutropenia. If WBC count declines, and especially if neutrophil count goes 1,000/mm3, expect to stop drug. If neutropenia is significant, also watch for evidence of infection and provide appropriate treatment, as prescribed.

PATIENT SAFTY

Instruct patient to take tablet whole with liquid. Caution against chewing, splitting, or crushing it because it’s designed to release drug at a controlled rate.

Explain that shell of tablet will be eliminated in stool and that patient need not worry if he sees tablet in stool.

Urge patient to rise slowly from sitting or lying to minimize orthostatic hypotension.

Caution patient to avoid hazardous activities until CNS effects of drug are known.

Advise patient to avoid activities that may cause overheating, such as exercising strenuously, being exposed to extreme heat, or becoming dehydrated.

Category

Chemical class: Selective serotonin subtype 3 (5-HT3) receptor antagonist
Therapeutic class: Antiemetic

Pregnancy category: B

Indications

To prevent acute and delayed nausea and vomiting from chemotherapy
Adults. 0.5 mg 1 hr before chemotherapy. I.V. INJECTION
Adults. 0.25 mg over 30 sec about 30 min before start of chemotherapy. To prevent postoperative nausea and vomiting for up to 24 hr after surgery I.V. INJECTION
Adults. 0.75 mg over 10 sec immediately before induction of anesthesia.

Incompatibilities

Palonosetron shouldn’t be mixed with any other drug.

Contraindications

Hypersensitivity to palonosetron or its components

Side Efect

CNS: Anxiety, dizziness, drowsiness, fatigue, headache, insomnia, weakness
CV: Bradycardia, hypotension, prolonged QT interval, tachycardia
GI: Abdominal pain, constipation, diarrhea
SKIN: Dermatitis, pruritus, rash
Other: Hyperkalemia, hypersensitivity reaction, injection site reaction (burning, induration, discomfort, pain)

Cautions

Use palonosetron cautiously in patients Enterochromaffin cells Nerve impulse Vagus nerve Irritation Small intestine mucosa 5-HT3 receptor sites 5-HT3 5-HT3 5-HT3 5-HT3 5-HT3 Palonosetron

Mechanism of Action

Chemotherapy may induce nausea and vomiting by irritating the small intestine’s mucosa, causing mucosal enterochromaffin cells to release serotonin (5-HT3). The 5-HT3stimulates sympathetic receptors on afferent vagal nerve endings, and the vagus nerve causes the vomiting reflex. Palonosetron selectively blocks these 5-HT3receptors. By keeping the vagus nerve from inducing the vomiting reflex, drug reduces or prevents nausea and vomiting. It also may block 5-HT3receptors centrally, in the brain’s chemoreceptor trigger zone. who have or may develop prolonged cardiac conduction intervals—especially QT interval—such as those with congenital QT syndrome, hypokalemia, or hypomagnesemia; those taking a diuretic known to induce electrolyte abnormalities, an antiarrhythmic, or another drug that may prolong QT interval; and those who have received cumulative high-dose anthracycline therapy. With these patients, obtain a baseline ECG before giving palonosetron; repeat the ECG 15 minutes or 24 hours after giving drug, as ordered. Notify prescriber of any delayed conduction.

Flush I.V. line with normal saline solution before and after giving I.V. palonosetron.

Closely monitor any patient hypersensitive to other selective serotonin receptor antagonists for a similar reaction. If a reaction occurs, notify prescriber immediately.

PATIENT SAFTY

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to notify prescriber of any hypersensitivity reaction, such as rash or allergic dermatitis.

Category

Chemical class: Bisphosphonate
Therapeutic class: Antihypercalcemic, bone resorption inhibitor

Pregnancy category: D

Indications

To treat cancer-induced hypercalcemia that’s inadequately managed by oral hydration alone

IV

Adults. 60 to 90 mg over 2 to 24 hr as a single dose when corrected serum calcium level is 12 to 13.5 mg/dl; 90 mg over 2 to 24 hr when corrected serum calcium level is greater than 13.5 mg/dl. May be repeated as prescribed after 7 days if hypercalcemia recurs.
DOSAGE ADJUSTMENT For patients with renal failure, dosage is limited to 30 mg over 4 to 24 hr, as prescribed. For patients with cardiac or renal failure, drug is given in a smaller volume of fluid or at a slower rate, as prescribed. To treat moderate to severe Paget’s disease of bone

IV

Adults. 30 mg daily over 4 hr on 3 consecutive days for a total dose of 90 mg. Repeated as needed and tolerated. To treat osteolytic bone metastases of breast cancer

IV

Adults. 90 mg over 2 hr every 3 to 4 wk. To treat osteolytic bone metastases of multiple myeloma

IV

Adults. 90 mg over 4 hr every mo.

Mechanism of Action

Inhibits bone resorption, possibly by impairing attachment of osteoclast precursors to mineralized bone matrix, thus reducing the rate of bone turnover in Paget’s disease and osteolytic metastases. Pamidronate also reduces the flow of calcium from resorbing bone into bloodstream.

Incompatibilities

Don’t mix pamidronate with calciumcontaining infusion solutions, such as Ringer’s solution.

Contraindications

Hypersensitivity to pamidronate, other bisphosphonates, or their components

Interactions

calcium-containing preparations; vitamin D preparations, such as calcifediol and calcitriol: Antagonized pamidronate effects when used to treat hypercalcemia thalidomide: Increased risk of renal dysfunction in patients with multiple myeloma

Side Efect

CNS: Confusion, fever, psychosis, visual hallucinations
CV: Hypotension
EENT: Conjunctivitis
GI: Abdominal cramps, anorexia, GI bleeding, indigestion, nausea, vomiting
GU: Azotemia, focal segmental glomerulosclerosis, nephrotic syndrome, hematuria, renal toxicity leading to failure
HEME: Leukopenia, lymphopenia
MS: Bone pain, muscle spasms or stiffness,osteonecrosis (mainly of jaw)
RESP: Dyspnea
SKIN: Pruritus, rash
Other: Anaphylaxis, angioedema, flulike symptoms, hyperkalemia, hypernatremia, hypocalcemia, hypokalemia, hypomagnesemia, hypophosphatemia, injection site pain and swelling, reactivation of herpes simplex and zoster infections

Cautions

Make sure patient has had a dental checkup before invasive dental procedures during pamidronate therapy, especially if he has cancer; is receiving chemotherapy, head or neck radiation, or a corticosteroid; or has poor oral hygiene. Risk of osteonecrosis is increased in these patients.
WARNING Don’t give more than 90 mg at any one time because of increased risk of serious adverse effect on kidneys.

Monitor patient for hypocalcemia, especially if patient has had thyroid surgery.

Stay alert for fever during first 3 days of therapy, especially in patients receiving high doses. If fever develops, obtain patient’s CBC with differential, as ordered.

Obtain serum creatinine level before each treatment. Notify prescriber of abnormal results because drug may need to be withheld or dosage adjusted until creatinine level returns to normal.

Assess patient with anemia, leukopenia, or thrombocytopenia for worsening of the condition during first 2 weeks of therapy.

PATIENT SAFTY

Stress need to comply with prescribed administration schedule for pamidronate.

Advise patient to avoid calcium and vitamin D supplements during therapy.

Instruct patient on proper oral hygiene and on need to notify prescriber about invasive dental procedures.

Category

Chemical class: Pancreatic enzyme
Therapeutic class: Digestant, pancreatic enzyme replacement

Pregnancy category: C

Indications

To treat pancreatic insufficiency, including steatorrhea ,
Adults. 8,000 to 24,000 units of lipase with meals or snacks, adjusted as prescribed, according to need for steatorrhea control. For severe insufficiency, up to 36,000 units of lipase with meals or snacks.

Mechanism of Action

Releases the enzymes pancreatin, lipase, amylase, and protease, mainly in the duodenum and upper jejunum. These enzymes facilitate the hydrolysis of fats into glycerol and fatty acids, starches into dextrins and sugars, and proteins into peptides. Pancreatin acts locally in the GI tract but is quickly inactivated by gastric acid.

Contraindications

Acute exacerbation of chronic pancreatic disease; acute pancreatitis; hypersensitivity to pancreatin, pancrelipase, or pork

Interactions

acarbose, miglitol: Decreased effectiveness of these aluminum hydroxide, H2-receptor antagonists, omeprazole, sodium bicarbonate: Increased gastric pH, prolonged enzymatic action of pancreatin calcium carbonate– and magnesium hydroxide–containing antacids: Decreased pancreatin effectiveness iron supplements: Decreased iron absorption

Side Efect

EENT: Stomatitis
GI: Abdominal cramps or pain, diarrhea, intestinal obstruction, nausea pancreatin 788
SKIN: Rash, urticaria
Other: Hyperuricemia

Cautions

WARNING Don’t administer pancreatin to patient who is allergic to pork.

Assess patient for GI disturbances and hyperuricemia when giving high doses of pancreatin.

If patient opens capsules and sprinkles contents on food, watch for signs or symptoms of sensitization (chest tightness, dyspnea, nasal congestion, wheezing), which may result from repeated inadvertent inhalation of powder.

Be aware that brands of pancreatin aren’t interchangeable because the same doses don’t contain equivalent amounts of drug.

PATIENT SAFTY

Instruct patient to take pancreatin before or with meals or snacks to maximize effectiveness.

To prevent capsule or tablet from lodging in esophagus, advise patient to take drug with a beverage while sitting upright, to swallow it quickly, and to follow with 1 or 2 mouthfuls of solid food.

Caution patient not to chew tablets; doing so may irritate mouth, lips, and tongue.

If patient has trouble swallowing capsules, advise her to open capsule and sprinkle its contents on food without inhaling them.

Caution patient not to take antacids that contain calcium carbonate or magnesium hydroxide during therapy.

Category

Chemical class: Porcine pancreatic enzyme
Therapeutic class: Pancreatic enzyme replacement

Pregnancy category: C

Indications

To treat pancreatic insufficiency, including steatorrhea , DELAYED-RELEASE , POWDER, Adults and adolescents. 33,000 to 44,000 units of lipase before or with meals or snacks; adjusted as prescribed. For patients with severe deficiency, possibly up to 88,000 units of lipase with meals or snacks or dosing frequency increased to every hr. Children ages 7 to 12. 4,000 to 12,000 units of lipase with meals and snacks; adjusted as needed and tolerated. Children ages 1 to 6. 4,000 to 8,000 units of lipase with meals and 4,000 units of lipase with each snack; adjusted as needed and tolerated. Infants ages 6 to 11 months. 2,000 units of lipase with meals; adjusted as needed and tolerated.

Mechanism of Action

Releases high levels of the enzymes lipase, amylase, and protease, mainly in duodenum and upper jejunum. These enzymes facilitate hydrolysis of fats into glycerol and fatty acids, starches into dextrins and sugars, and proteins into peptides.

Contraindications

Acute exacerbation of chronic pancreatic disease; acute pancreatitis; hypersensitivity to pancreatin, pancrelipase, or pork

Interactions

acarbose, miglitol: Decreased effectiveness of these aluminum hydroxide, H2-receptor antagonists, omeprazole, sodium bicarbonate: Increased gastric pH, prolonged enzymatic action of pancrelipase calcium carbonate– and magnesium hydroxide–containing antacids: Decreased pancrelipase effectiveness iron supplements: Decreased iron absorption

Side Efect

EENT: Stomatitis
GI: Abdominal cramps or pain, diarrhea, intestinal obstruction, nausea
HEME: Anemia
SKIN: Rash, urticaria
Other: Hyperuricemia

Cautions

WARNING Don’t administer pancrelipase to patient who is allergic to pork.

Be aware that brands of pancrelipase aren’t interchangeable because the same doses don’t contain equivalent amounts of drug.

Mix powder with fluid or soft, nondairy food.

If needed, open delayed-release capsules and mix contents (enteric-coated spheres, microspheres, or microtablets) with liquid or soft food that requires no chewing. Give immediately because enteric coating will dissolve after prolonged contact with at a pH greater than 6.

If patient opens capsules and sprinkles contents on food, assess for signs of sensitization (chest tightness, dyspnea, nasal congestion, wheezing), which may result from repeated inadvertent inhalation of powder.

Give drug before or with meals and snacks, and follow with a glass of water or juice.

Expect drug to cause stomatitis if held in mouth.

Check stool for fecal fat content, as ordered.

Monitor patient for iron deficiency anemia because serum iron level may decline during pancrelipase therapy.

PATIENT SAFTY

Instruct patient to take pancrelipase before or with meals and snacks and to follow with a glass of water or juice.

Instruct patient not to chew capsules (or capsule contents) or crush tablets and to swallow immediately because drug may cause irritation if held in mouth.

Urge patient not to inhale powder from delayed-release capsules; doing so may cause chest tightness, shortness of breath, stuffy nose, trouble breathing, and wheezing.

Inform patient that sneezing and tearing also may result from contact with powder.

Caution patient not to use antacids; they may decrease drug effectiveness.

Inform patient that her stool may have foul smell.

Category

Chemical class: Substituted benzimidazole
Therapeutic class: Antiulcer, gastric acid proton pump inhibitor

Pregnancy category: B

Indications

To treat gastroesophageal reflux disease (GERD) DELAYED-RELEASE
Adults. 40 mg daily for up to 8 wk. Repeated for another 4 to 8 wk if healing doesn’t occur.

IV

Adults. 40 mg daily infused over 2 min or 15 min for 7 to 10 days, followed by oral doses. To maintain healing of erosive esophagitis and reduce relapse of daytime and nighttime symptoms in patients with GERD DELAYED-RELEASE
Adults. 40 mg daily for up to 12 mo. To treat pathological hypersecretion associated with Zollinger-Ellison syndrome or other neoplastic conditions

IV

Adults. 80 mg every 12 hr infused over 2 min or 15 min; adjusted based on patient’s acid output measurements up to 80 mg every 8 hr. Route Onset Peak Duration P.O. 1 day 1 wk 1 wk I.V. 1 day Unknown 1 wk

Mechanism of Action

Interferes with gastric acid secretion by inhibiting the hydrogen-potassiumadenosine triphosphatase (H+-K+-ATPase) enzyme system, or proton pump, in gastric parietal cells. Normally, the proton pump uses energy from hydrolysis of ATPase to drive H+and chloride (Cl–) out of parietal cells and into the stomach lumen in exchange for potassium (K+), which leaves the stomach lumen and enters parietal cells. After this exchange, H+and Cl–combine in the stomach to form hydrochloric acid (HCl). Pantoprazole irreversibly inhibits the final step in gastric acid production by blocking the exchange of intracellular H+ and extracellular K+, thus preventing H+ from entering the stomach and additional HCl from forming.

Incompatibilities

Midazolam and products containing zinc may cause precipitation or discoloration.

Contraindications

Hypersensitivity to pantoprazole, substituted benzimidazoles (omeprazole, lansoprazole, rabeprazole sodium), or their components

Interactions

ampicillin, cyanocobalamin, digoxin, iron salts,
ketoconazole: Possibly impaired absorption of these atazanavir: Significantly decreased atazanavir level
warfarin: Increased INR, PT, and bleeding risk

Side Efect

CNS: Anxiety, asthenia, confusion, dizziness, headache, hypertonia, hypokinesia, insomnia, malaise, migraine, speech disorder vertigo
CV: Chest pain, hypercholesterolemia, hyperlipidemia
EENT: Anterior ischemic optic neuropathy, blurred vision, increased salivation, pharyngitis, rhinitis, sinusitis, tinnitus
ENDO: Hyperglycemia
GI: Abdominal pain, atrophic gastritis, constipation, diarrhea, elevated liver function tests results, flatulence, gastroenteritis, hepatotoxicity, indigestion, nausea, pancreatitis, vomiting
GU: Elevated serum creatinine level, interstitial nephritis
HEME: Pancytopenia
MS: Arthralgia, back or neck pain, rhabdomyolysis
RESP: Bronchitis, dyspnea, increased cough, upper respiratory tract infection
SKIN: Erythema multiforme, rash, StevensJohnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, angioedema, elevated creatine kinase and phosphokinase levels, flulike symptoms, generalized pain, hyperuricemia, infection, injection site reaction

Cautions

Ensure the continuity of gastric acid suppression during transition from oral to I.V. pantoprazole (or vice versa) because even a brief interruption of effective suppression can lead to serious complications.

Don’t give pantoprazole within 4 weeks of testing for Helicobacter pylori because antibiotics, proton pump inhibitors, and bismuth preparations suppress H. pylori and may lead to false-negative results. Drug also may cause false-positive results in urine screening tests for tetrahydrocannabinol. Consult guidelines for pantoprazole use before testing.

Flush I.V. line with D5W, normal saline solution, or lactated Ringer’s injection before and after giving drug.

When giving I.V. over 2 minutes, reconstitute with 10 ml of normal saline injection. Solution may be stored up to 2 hours at room temperature.

When giving I.V. over 15 minutes, reconstitute with 10 ml normal saline injection. Then, further reconstitute with 100 ml (for GERD) or 80 ml (for pathological hypersecretion in Zollinger-Ellison syndrome) of D5W, normal saline injection, or lactated Ringer’s injection. Solution may be stored up to 2 hours before further dilution and up to 22 hours before use.

Expect to monitor PT or INR during therapy if patient takes an oral anticoagulant.

If therapy lasts more than 3 years, patient may not be able to absorb vitamin B12 because of hypochlorhydria or achlorhydria. Treatment for cyanocobalamin deficiency may be needed.

PATIENT SAFTY

Instruct patient to swallow pantoprazole tablets whole and not to chew or crush them.

Advise patient to expect relief of symptoms within 2 weeks of starting therapy.

Advise patient who takes warfarin to follow bleeding precautions and to notify prescriber immediately if bleeding occurs.

Category

Chemical class: Sterol derivative, vitamin D analogue
Therapeutic class: Antihyperparathyroid

Pregnancy category: Not rated

Indications

To prevent and treat secondary hyperparathyroidism in patients with chronic renal failure stage 3 or 4 I.V. INJECTION
Adults. Initial: 0.04 to 0.1 mcg/kg (2.8 to 7 mcg) no more than every other day at any time during dialysis. Maintenance: If initial dosage doesn’t produce a satisfactory response, 2 to 4 mcg given every 2 to 4 wk. Maximum: 0.24 mcg/kg/dose or up to 16.8 mcg/dose. Children age 5 and over.Initial: 0.04 mcg/ kg three times weekly if baseline intact parathyroid hormone (iPTH) level is less than 500 pg/ml, or 0.08 mcg/kg three times weekly if baseline iPTH level equals or exceeds 500 pg/ml. Maintenance: If initial dosage isn’t adequate, adjust in 0.04-mcg/kg increments as needed.
DOSAGE ADJUSTMENT If serum PTH level remains the same or increases, dosage is increased. If PTH level decreases by less than 30%, dosage is increased. If PTH level decreases by 30% to 60%, dosage is maintained. If PTH level decreases by more than 60%, dosage is decreased. If PTH level is 1.5 to 3 times the upper limit of normal, dosage is maintained.
DOSAGE ADJUSTMENT Dosage is immediately reduced or drug stopped if serum calcium level is elevated or serum calciumphosphorus product exceeds 75. Dosage restarted at a lower dose when these levels return to normal.
Adults. Initial: If baseline iPTH level is less than 500 pg/ml, 1 mcg daily or 2 mcg three times weekly, doses separated by at least 1 day. If iPTH level exceeds 500 pg/ml, 2 mcg daily or 4 mcg three times weekly, doses separated by at least 1 day. Maintenance: Dosage adjusted in 1-mcg increments based on iPTH level relative to baseline. Route Onset Peak Duration I.V. Unknown Unknown 15 hr

Mechanism of Action

Reduces serum PTH level by an unknown mechanism. In chronic renal failure, decreased renal synthesis of vitamin D leads to chronic hypocalcemia. In response, parathyroid glands secrete PTH to stimulate vitamin D synthesis, but serum calcium levels can’t normalize because of renal failure.

Contraindications

Evidence of vitamin D toxicity,hypercalcemia,hypersensitivity to paricalcitol or components

Interactions

atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole: Increased effects of oral paricalcitol , such as cholestyramine, that impair absorption of fat-soluble vitamins: Possibly impaired absorption of oral paricalcitol

Side Efect

CNS: Arthritis, asthenia, chills, depression, dizziness, fever, headache, insomnia, lightheadedness, malaise, neuropathy, syncope, vertigo
CV: Cardiomyopathy, chest pain, congestive heart failure, edema, hypertension, hypotension, MI, orthostatic hypotension, palpitations
EENT: Amblopia, bronchitis, dry mouth, epistaxis, laryngeal edema, pharyngitis, retinal abnormality, rhinitis, sinusitis, taste perversion
ENDO: Hypoglycemia
GI: Abdominal pain, constipation, diarrhea, dyspepsia, gastritis, gastroenteritis, GI bleeding, nausea, vomiting
GU: Abnormal kidney function, uremia, UTI
MS: Back pain, leg cramps, myalgia
RESP: Increased cough, pneumonia
SKIN: Ecchymosis, hypertrophy, pruritus, rash (including vesiculobullous), ulceration, urticaria
Other: Acidosis, allergic reaction, angioedema, dehydration, generalized edema, gout, hyperkalemia, hyperphosphatemia, hypervolemia, hypokalemia, infections, influenza, sepsis

Cautions

Before giving drug, look for particles and discoloration; if present, discard drug.

Give as I.V. bolus; discard unused portion.

Monitor serum calcium and phosphorus levels, as ordered, twice weekly to guide
DOSAGE ADJUSTMENTs and then monthly.
WARNING Paricalcitol may lead to vitamin D toxicity and hypercalcemia. Early evidence includes arthralgia, constipation, dry mouth, headache, metallic taste, myalgia, nausea, somnolence, vomiting, and weakness. Late evidence includes albuminuria, anorexia, arrhythmias, azotemia, conjunctivitis (calcific), decreased libido, elevated BUN and serum ALT and AST levels, vascular calcification, hypercholesterolemia, hypertension, hyperthermia, irritability, mild acidosis, nephrocalcinosis, nocturia, pancreatitis, photophobia, polydipsia, polyuria, pruritus, rhinorrhea, and weight loss.

If toxicity occurs, notify prescriber immediately and expect to decrease or stop drug. Place patient on bed rest and give fluids, low-calcium diet, and a laxative, as prescribed. If patient has a hypercalcemic crisis and dehydration, expect to infuse normal saline solution and a loop diuretic to prompt renal calcium excretion.

Expect to check patient’s serum PTH level every 3 months.

If patient also takes digoxin, monitor her for evidence of digitalis glycoside toxicity, which is potentiated by hypercalcemia.

Store drug at 25° C (77° F).

PATIENT SAFTY

Advise patient to follow a diet high in calcium and low in phosphorus.

Explain that phosphate binders may be needed to control serum phosphorus level.

Review early evidence of hypercalcemia and vitamin D toxicity. Tell patient to contact prescriber immediately if it develops.

Urge patient to avoid hazardous activities until drug’s CNS effects are known.

If patient takes digoxin, explain evidence of toxicity and the need to contact prescriber immediately if it develops.

Category

Chemical class: Phenylpiperidine derivative
Therapeutic class: Antidepressant, antiobsessional, antipanic

Pregnancy category: D

Indications

To treat major depression C.R.
Adults. Initial: 25 mg daily, increased as prescribed and tolerated by 12.5 mg daily every wk. Maximum: 62.5 mg daily. ORAL SUSPENSION,
Adults. Initial: 20 mg daily, increased as prescribed and tolerated by 10 mg daily every wk. Maximum: 50 mg daily. To treat obsessive-compulsive disorder ORAL SUSPENSION,
Adults. Initial: 20 mg daily, increased as prescribed and tolerated by 10 mg daily every wk. Usual: 20 to 60 mg daily. Maximum: 60 mg daily. To treat panic disorder C.R.
Adults. Initial: 12.5 mg daily, increased by 12.5 mg daily every wk as needed. Maximum: 75 mg daily. ORAL SUSPENSION,
Adults. Initial: 10 mg daily, increased as prescribed and tolerated by 10 mg daily every wk. Usual: 10 to 60 mg daily. Maximum: 60 mg daily. To treat social anxiety disorder C.R.
Adults. Initial: 12.5 mg daily, increased by 12.5 mg daily every wk as needed. Maximum: 37.5 mg daily. ORAL SUSPENSION, (HYDROCHLORIDE)
Adults. Initial: 20 mg daily, increased as prescribed and tolerated by 10 mg daily every wk. Usual: 20 to 60 mg daily. Maximum: 60 mg daily. To treat generalized anxiety disorder ORAL SUSPENSION, (HYDROCHLORIDE)
Adults. Initial: 20 mg daily, increased as prescribed and tolerated by 10 mg daily every wk. Usual: 20 to 50 mg daily. Maximum: 60 mg daily. To treat posttraumatic stress disorder ORAL SUSPENSION, (HYDROCHLORIDE)
Adults. Initial: 20 mg daily, increased as prescribed and tolerated by 10 mg daily every wk. Usual: 20 to 50 mg daily. Maximum: 50 mg daily. To treat premenstrual dysphoric disorder C.R.
Adults. Initial: 12.5 mg daily in the morning, increased as needed after 1 wk to 25 mg daily. Or, 12.5 mg daily in the morning only during luteal phase of menstrual cycle (2-wk period before onset of monthly cycle), increased as needed after 1 wk to 25 mg daily in the morning during luteal phase of menstrual cycle.
DOSAGE ADJUSTMENT For patients who are elderly, debilitated, or have creatinine clearance less than 30 ml/min/1.73 m2, initially 10 mg daily; maximum, 40 mg daily. Avoid C.R. form. For patients taking C.R. tablets with creatinine clearance less than 30 ml/ min/1.73 m2, initially 12.5 mg daily; maximum, 50 mg daily. Route Onset Peak Duration P.O. 1–4 wk Unknown Unknown

Mechanism of Action

Exerts antidepressant, antiobsessional, and antipanic effects by potentiating serotonin activity in CNS and inhibiting serotonin reuptake at presynaptic neuronal membrane. Blocked serotonin reuptake increases levels and prolongs activity of serotonin at synaptic receptor sites.

Contraindications

Hypersensitivity to paroxetine or its components,pimozide therapy,use within 14 days of an MAO inhibitor,thioridazine therapy

Interactions

antacids: Hastened release of C.R. paroxetine aspirin, NSAIDs,
warfarin: Increased anticoagulant activity and risk of bleeding astemizole: Increased risk of arrhythmias atomoxetine; risperidone; other metabolized by CYP2D6, such as amitriptyline, desipramine, fluoxetine, imipramine, phenothiazines, tamoxifen, type IC antiarrhythmics: Increased plasma levels of these barbiturates, primidone: Decreased blood paroxetine level
cimetidine: Possibly increased blood paroxetine level cisapride, isoniazid, MAO inhibitors, procarbazine: Possibly serotonin syndrome codeine, haloperidol, metoprolol, perphenazine, propranolol, risperidone, thioridazine: Decreased metabolism and increased effects of these cyproheptadine: Decreased paroxetine effects dextromethorphan: Decreased dextromethorphan metabolism and increased risk of toxicity digoxin: Possibly decreased digoxin effects encainide, flecainide, propafenone,
quinidine: Potentiated toxicity of these fosamprenavir, ritonavir: Decreased plasma paroxetine level lithium: Possibly increased blood paroxetine level, increased risk of serotonin syndrome methadone: Decreased methadone metabolism, increased risk of adverse effects
phenytoin: Possibly phenytoin toxicity pimozide: Increased risk of prolonged QT interval procyclidine: Increased blood procyclidine level and anticholinergic effects serotonergic such as linezolid, St. John’s wort, tramadol, triptans, and tryptophan: Increased risk of serotonin syndrome tamoxifen: Decreased tamoxifen effectiveness
theophylline: Possibly increased blood theophylline level and risk of toxicity thioridazine: Increased thioridazine level, possibly leading to prolonged QT interval and life-threatening ventricular arrhythmias
tramadol: Increased risk of serotonin syndrome and seizures tricyclic antidepressants: Increased metabolism and blood antidepressant levels; increased risk of toxicity, including seizures

Side Efect

CNS: Agitation, akathisia, asthenia, confusion, decreased concentration, dizziness, drowsiness, emotional lability, hallucinations, headache, insomnia, mania, neuroleptic malignant syndrome, psychomotor agitation, restlessness, serotonin syndrome, somnolence, suicidal ideation, tremor
CV: Palpitations, tachycardia
EENT: Blurred vision, dry mouth, rhinitis, taste perversion
GI: Abdominal cramps or pain, anorexia, constipation, diarrhea, flatulence, nausea, vomiting
GU: Decreased libido, difficult ejaculation, impotence, sexual dysfunction, urine retention
MS: Back pain, myalgia, myasthenia, myopathy
SKIN: Diaphoresis, rash
Other: Weight gain or loss

Cautions

Shake oral suspension well. Measure with an oral syringe or calibrated device.

Don’t give enteric-coated form with antacids.

Watch for akathisia (inner sense of restlessness) and psychomotor agitation, especially during the first few weeks of therapy.

Watch patient closely (especially children, adolescents, and young adults), for suicidal tendencies, particularly when therapy starts and dosage changes, because depression may worsen temporarily during these times, possibly leading to suicidal ideation.

Watch for mania, which may result from any antidepressant in a susceptible patient.

Monitor patient closely for evidence of GI bleeding, especially if patient also takes a drug known to cause GI bleeding, such as aspirin, an NSAID, or warfarin.
WARNING Monitor patient closely for serotonin syndrome exhibited by agitation, hallucinations, coma, tachycardia, labile blood pressure, hyperthermia, hyperreflexia, incoordination, nausea, vomiting, or diarrhea. Notify prescriber immediately because serotonin syndrome may be lifethreatening, and provide supportive care.
WARNING Be aware that serotonin syndrome in its most severe form may resemble neuroleptic malignant syndrome, which includes hyperthermia, muscle rigidity, and autonomic instability with possibly rapid changes in vital signs and mental status. Stop drug immediately, and provide supportive care.

To minimize

Side Efect

, expect to taper drug rather than stopping abruptly.

PATIENT SAFTY

Advise patient to take paroxetine in the morning to minimize insomnia and to take it with food if adverse GI reactions develop.

Instruct patient to avoid taking C.R. paroxetine within 2 hours of an antacid.

Tell patient to swallow C.R. tablets whole and not to cut, crush, or chew them.

Suggest that patient avoid hazardous activities until drug’s CNS effects are known.

Tell family or caregiver to observe patient closely for suicidal tendencies, especially when therapy starts or dosage changes and especially if patient is a child, teenager, or young adult.

Explain that full effect may take 4 weeks.

Urge patient to avoid alcohol during therapy; effects with paroxetine are unknown. paroxetine 795 P

Tell patient not to take aspirin or NSAIDs during therapy because they increase the risk of bleeding. If patient takes warfarin, tell her to use bleeding precautions and to notify prescriber at once if bleeding occurs.

Inform patient that episodes of acute depression may persist for months or longer and that they require continued follow-up.

Instruct patient not to stop drug abruptly but to taper dosage as instructed.

Alert female patients of childbearing age that paroxetine may cause birth defects and persistent pulmonary hypertension in the newborn if taken during the first trimester of pregnancy. Stress the need for effective contraception and to notify prescriber if pregnancy occurs or is suspected.

Caution patient to alert all prescribers about paroxetine therapy because of potentially serious drug interactions.

Category

Chemical class: Recombinant granulocyte colony-stimulating factor conjugate
Therapeutic class: Antineutropenic, hematopoietic stimulator

Pregnancy category: C

Indications

To reduce the risk of infection, as manifested by febrile neutropenia, after myelosuppressive chemotherapy SUBCUTANEOUS INJECTION
Adults. 6 mg with each chemotherapy cycle.

Mechanism of Action

Induces formation of neutrophil progenitor cells by binding to receptors on granulocytes, which then divide. Pegfilgrastim also potentiates the effects of mature neutrophils, thus reducing fever and the risk of infection from severe neutropenia. It is pharmacologically identical to human granulocyte colony-stimulating factor.

Contraindications

Hypersensitivity to filgrastim, pegfilgrastim, or their components or to proteins derived from Escherichia coli

Interactions

lithium: Increased neutrophil production

Side Efect

CNS: Fever
GI: Elevated liver function test results, splenic rupture, splenomegaly
GU: Elevated uric acid level
HEME: Leukocytosis, sickle cell crisis
MS: Bone pain
RESP: Acute respiratory distress syndrome, dyspnea, hypoxia, pulmonary infiltrates
SKIN: Acute febrile neutrophilic dermatosis (Sweet’s syndrome), erythema, flushing, rash, urticaria
Other: Anaphylaxis, angioedema, antibody formation to pegfilgrastim, injection site reactions (pain, induration, erythema)

Cautions

Avoid giving pegfilgrastim for 14 days before and 24 hours after cytotoxic chemotherapy.

Check CBC, hematocrit, and platelet count before and periodically during therapy.

Let drug warm to room temperature before injection. Use prefilled syringe and needles.

Don’t shake the solution.

Discard drug that contains particles, is discolored, or was stored more than 48 hours at room temperature.
WARNING If signs of allergy occur, stop pegfilgrastim infusion and notify prescriber at once. If anaphylaxis occurs, give antihistamine, epinephrine, corticosteroid, and bronchodilator, as ordered.
WARNING Patients receiving filgrastim (parent drug) have had splenic rupture and acute respiratory distress syndrome. Assess patient for fever, respiratory distress, and upper abdominal or shoulder tip pain.

Assess patients with sickle cell disease for signs of sickle cell crisis; urge hydration.

Give nonopioid and opioid analgesics, as ordered, if patient experiences bone pain.

Store drug at 2° to 8° C (36° to 46° F), and protect from freezing and light.

Be aware that needle cover contains dry natural rubber and should not be handled by persons with a latex allergy.

PATIENT SAFTY

Urge patient to promptly report possibly serious reactions (trouble breathing, rash, chest tightness, left upper abdominal pain, shoulder tip pain) and evidence of infection (fever, chills).

If patient will self-administer, teach her how to prepare, give, and store drug.

Alert her that needle cover contains dry natural rubber and should not be handled if she has a latex allergy.

Tell patient to rotate injection sites among thigh, abdomen (except for 2 inches around navel), buttocks, and outer, upper arms. Caution her to avoid tender, hard, red, or bruised areas.

Urge patient to discard used needles and syringes in a puncture-resistant container and not to reuse them.

Stress the importance of follow-up tests.

Advise patient to store pegfilgrastim in refrigerator and not to freeze it. Tell her to discard drug if left unrefrigerated for more than 48 hours.

Category

Chemical class: Human growth hormone (GH) receptor antagonist
Therapeutic class: Growth suppressant

Pregnancy category: B

Indications

To treat acromegaly in patients with an inadequate response to surgery, radiation, or other medical treatment or for whom such treatment is inappropriate SUBCUTANEOUS INJECTION
Adults. Initial: 40 mg as loading dose on day 1; then 10 mg daily. Maintenance: Adjusted every 4 to 6 wk in 5-mg increments if insulin-like growth factor-I (IGF-I) levels are abnormal. Maximum: 30 mg daily.

Contraindications

Hypersensitivity to pegvisomant, its components, or latex

Interactions

insulin, oral antidiabetics: Enhanced action of insulin and oral antidiabetics, possibly resulting in hypoglycemia opioids: Decreased pegvisomant level

Side Efect

CNS: Dizziness, paresthesia
CV: Chest pain, hypertension, peripheral edema
EENT: Ear infection, sinusitis
GI: Diarrhea, elevated liver function test results, nausea
MS: Back pain
RESP: Upper respiratory tract infection
SKIN: Blisters
Other: Cold, flulike symptoms, injection site lipohypertrophy and pain, weight gain

Cautions

Obtain liver enzyme levels before starting pegvisomant, as ordered. If they’re elevated but 3 times or less normal, expect to monitor them monthly for 6 months, quarterly for 6 months, and then twice yearly for the next year. If they’re more than 3 times normal, expect to withhold drug until the cause of elevation has been determined.

Reconstitute drug by injecting 1 ml of diluent provided (sterile water for injection) into vial, aiming the stream against vial wall. Hold vial between the palms of both hands and roll gently to dissolve powder. Don’t shake. Give within 6 hours of reconstitution, and discard any remaining amount.

Watch for evidence of liver dysfunction during therapy. If liver enzyme levels rise to 3 to 5 times normal but patient has no evidence of liver dysfunction (jaundice, bilirubinuria, fatigue, nausea, vomiting, right-upper-quadrant pain, ascites, unexplained edema, easy bruising) or increases in serum total bilirubin level, expect therapy to continue but liver enzymes to be monitored weekly and a complete hepatic workup to be done. If enzyme levels are at least 5 times above normal or transaminase level is at least 3 times above normal with increased total bilirubin (with or without evidence of hepatic dysfunction), notify prescriber immediately and expect to stop drug. If patient develops evidence of hepatic dysfunction, regardless of liver enzyme levels, notify prescriber immediately, and expect a complete liver workup to be performed. If liver damage is conpegvisomant 797 P firmed, expect drug to be stopped.

Monitor patient’s IGF-1 levels every 4 to 6 weeks, as ordered, until they’ve normalized and then every 6 months. Notify prescriber if levels are decreased or elevated. Be aware that GH levels should not be used to make
DOSAGE ADJUSTMENTs because pegvisomant interferes with laboratory measurement of GH.

PATIENT SAFTY

Teach patient how to reconstitute and administer pegvisomant.

Tell patient about the need for frequent laboratory studies and their importance to properly adjust drug dosage and detect drug-related abnormalities.

Advise patient to stop drug immediately and notify prescriber if her skin or whites of her eyes become yellow or she has other evidence of liver dysfunction, such as dark urine, light-colored stools, little or no appetite for several days, nausea, tiredness, or abdominal pain.

Instruct woman of childbearing age to report known or suspected pregnancy.

Caution patient to tell prescriber about all other she’s taking.

Category

Chemical class: Nonselective betaadrenergic blocker
Therapeutic class: Antihypertensive

Pregnancy category: Not rated

Indications

To manage hypertension
Adults. 20 mg daily.
DOSAGE ADJUSTMENT For elderly patients, dosage individualized according to sensitivity to drug. Route Onset Peak Duration P.O. Unknown 1.5–3 hr Unknown

Mechanism of Action

May reduce blood pressure by competing with beta-adrenergic receptor agonists, which helps reduce cardiac output, decrease sympathetic outflow to peripheral blood Blood vessel Blood vessel Blood stream Blood stream IGF-1 IGF-1 IGF-1 IGF-1 IGF-1 IGF-1 IGF-1 IGF-1 GH GH GH GH GH receptors Cell membrane GH receptors Pegvisomant Cell membrane Blood vessel Blood vessel Blood stream Blood stream IGF-1 IGF-1 IGF-1 IGF-1 IGF-1 IGF-1 IGF-1 IGF-1 GH GH GH GH GH receptors Cell membrane GH receptors Pegvisomant Cell membrane

Mechanism of Action

In acromegaly, elevated blood levels of growth hormone (GH) overstimulate the liver to produce excessive amounts of insulin-like growth factors (IGFs), such as IGF-1. Excessive IGFs before puberty stimulate the linear growth of bones, causing the patient’s unusual height and extremely long arms and legs. After puberty, the excessive hormone secretion causes periosteal bone proliferation, resulting in widening of the hands and feet, and coarsening of the facial features, as well as other complications. Pegvisomant selectively blocks GH cell surface receptors. As a result, the liver delivers less IGF-1 and other proteins to the blood, preventing the overgrowth of bone and other tissues. vessels, and inhibit renin release by kidneys.

Contraindications

Asthma, bradycardia (fewer than 45 beats/ min), cardiogenic shock, heart failure, hypersensitivity to penbutolol or its components, secondor third-degree AV block

Interactions

allergen immunotherapy, allergenic extracts for skin testing: Increased risk of serious systemic reaction or anaphylaxis amiodarone: Additive depressant effect on cardiac conduction, negative inotropic effects anesthetics (hydrocarbon inhalation): Increased risk of myocardial depression and hypotension calcium channel blockers, clonidine, diazoxide, guanabenz, other hypotension-producing , reserpine: Additive hypotension and possibly other beta blocker effects
cimetidine: Possibly increased blood penbutolol level estrogens: Decreased antihypertensive effect of penbutolol fentanyl and its derivatives: Possibly increased risk of initial bradycardia after induction doses of fentanyl derivative (with long-term penbutolol use) insulin, oral antidiabetic : Possibly impaired glucose control and masking of hypoglycemia symptoms such as tachycardia lidocaine: Decreased lidocaine clearance, increased risk of lidocaine toxicity
MAO inhibitors: Increased risk of significant hypertension neuromuscular blockers: Possibly potentiated and prolonged action of these
NSAIDs: Possibly decreased hypotensive effect of penbutolol other
beta blockers: Additive beta blocker effects phenothiazines: Increased blood levels of both phenytoin (parenteral): Additive cardiac depressant effects sympathomimetics, xanthines: Possibly inhibited effects of penbutolol and these

Side Efect

CNS: Anxiety, depression, dizziness, drowsiness, fatigue, insomnia, light-headedness, nervousness, syncope, weakness
CV: Bradycardia, chest pain, edema, peripheral vascular insufficiency
EENT: Nasal congestion
GI: Constipation, diarrhea, epigastric pain, nausea, vomiting
GU: Impotence
RESP: Bronchospasm, dyspnea

Cautions

Expect varied drug effectiveness in elderly patients, who may be more sensitive to antihypertensive effects because of reduced drug clearance by kidneys.
WARNING Avoid stopping penbutolol abruptly because doing so may precipitate MI, myocardial ischemia, severe hypertension, or ventricular arrhythmias, particularly in patients with cardiovascular disease. Watch for tachycardia because drug also may mask some signs of hyperthyroidism. Abrupt withdrawal of drug in patients with hyperthyroidism or thyrotoxicosis can precipitate thyroid storm.

Monitor blood pressure and cardiac output, as appropriate, in patients who have a history of systolic heart failure or left ventricular dysfunction. Drug’s negative inotropic effect can depress cardiac output.

Monitor patients with diabetes mellitus who take antidiabetics because penbutolol can prolong hypoglycemia or promote hyperglycemia. It also can mask evidence of hypoglycemia, especially tachycardia, palpitations, and tremor.

Watch for impaired circulation in elderly patients with age-related peripheral vascular disease or patients with Raynaud’s phenomenon. Elderly patients are also at increased risk for beta blocker–induced hypothermia.

Monitor drug refill frequency to help determine patient compliance.

PATIENT SAFTY

Instruct patient to take penbutolol at the same time every day and not to change dosage without consulting prescriber.

Advise patient not to stop taking drug abruptly, but to taper dosage gradually under prescriber’s supervision.

Instruct patient with diabetes mellitus to regularly monitor blood glucose level and test urine for ketones.

Advise patient to consult prescriber before taking OTC , especially cold products.

Urge patient to avoid hazardous activities until CNS effects of drug are known.

Instruct patient to inform prescriber of chest pain, fainting, light-headedness, or shortness of breath, any of which may indicate the need for a dosage change.

Inform patient that penbutolol doesn’t cure hypertension. Encourage her to follow recommended diet and lifestyle changes.

Category

Chemical class: Degradation product of penicillin
Therapeutic class: Antirheumatic, antiurolithic, chelating agent

Pregnancy category: D

Indications

To treat cystinuria , Adults and adolescents. 500 mg q.i.d. Children. 7.5 mg/kg q.i.d. To treat rheumatoid arthritis , Adults and adolescents.Initial: 125 or 250 mg daily. Dosage increased by 125 or 250 mg daily every 2 to 3 mo. Maximum: 1,500 mg daily. To treat Wilson’s disease , Adults and adolescents. Dosage individualized up to 2 g daily in divided doses q.i.d. by measuring urinary copper excretion.
DOSAGE ADJUSTMENT For elderly patients, 125 mg daily initially, then increased by 125 mg daily every 2 to 3 mo, up to maximum of 750 mg daily. For pregnant women, maximum dose of 1 g daily. For women having planned cesarean section, dosage limited to 250 mg daily during last 6 wk of pregnancy and until wound healing completed.

Mechanism of Action

Combines with copper to form a ringshaped complex that’s excreted in urine, thereby reducing copper levels in the body. Penicillamine also lowers urine cystine levels by binding with cystine to form penicillamine-cysteine disulfide, which is more soluble than cystine and more easily excreted in urine. The decrease in urine cystine level also helps prevent formation of cystine calculi and may help existing cystine calculi dissolve over time. In addition, penicillamine improves lymphocyte function by reducing IgM rheumatoid factor and immune complexes in serum and synovial fluid, which may play a role in treatment of rheumatoid arthritis. Route Onset Peak Duration P.O. 2–3 mo* Unknown Unknown

Contraindications

Hypersensitivity to penicillin, penicillamine, or their components; penicillaminerelated aplastic anemia or agranulocytosis; renal insufficiency (for patients with rheumatoid arthritis)

Interactions

4-aminoquinolines, bone marrow depressants, gold compounds, immunosuppressants (excluding glucocorticoids), phenylbutazone: Possibly increased risk of serious hematologic or renal

Side Efect

iron supplements: Possibly decreased effectiveness of penicillamine pyridoxine: Decreased effectiveness of pyridoxine, possibly increased risk of anemia or peripheral neuritis reaction

Side Efect

CNS: Agitation, anxiety, fever, mental changes, myasthenic syndrome, neuropathy
EENT: Altered or loss of taste, optic neuritis, stomatitis, tinnitus
GI: Anorexia, diarrhea, hepatic dysfunction, intrahepatic cholestasis, mild epigastric pain, pancreatitis, nausea, toxic hepatitis, vomiting
GU: Glomerulonephropathy, hematuria, proteinuria, renal failure
HEME: Agranulocytosis, aplastic anemia, hemolytic anemia, leukopenia, thrombocytopenia
MS: Arthralgia, dystonia, muscle weakness * For rheumatoid arthritis; 1 to 3 mo for Wilson’s disease.
SKIN: Pemphigus, pruritus, rash, urticaria
Other: Lupuslike symptoms, lymphadenopathy

Cautions

Use penicillamine cautiously in elderly patients because they’re at greater risk for rash, altered taste, and renal impairment.

Give penicillamine 1 hour before or 2 hours after meals and at least 1 hour before or after any other drug, food, or milk. Give last dose of day at least 3 hours after evening meal to maximize absorption.

For patient who has difficulty swallowing capsules or tablets, open capsule and mix contents in 15 to 30 ml of pureed fruit or fruit juice to mask drug’s sulfur odor. Alternatively, ask pharmacist to prepare elixir for oral administration.

Expect to give 25 mg pyridoxine, as prescribed, to patients receiving penicillamine because penicillamine increases intake requirements for this vitamin.

Watch for febrile reactions in patients who developed a fever during previous penicillamine therapy. Expect to stop drug if patient develops drug-induced fever.

Assess skin and mucous membranes for possible sensitivity reactions, such as skin lesions and mouth ulcers. Be prepared to discontinue drug as prescribed.

Expect to monitor urine laboratory test results twice weekly during first month of therapy, then every 2 weeks for next 5 months, and monthly thereafter. Watch for proteinuria or hematuria, which may precipitate nephrotic syndrome, especially in patients with renal disease or history of renal insufficiency. Also, weigh patient daily, watch for edema, and monitor intake and output because penicillamine may worsen underlying renal disease.
WARNING Monitor patient’s WBC and differential cell count, hemoglobin, and platelet count, as ordered, and assess skin, lymph nodes, and body temperature for abnormalities twice weekly during first month of therapy, then every 2 weeks for next 5 months, and monthly thereafter because drug may cause potentially serious hematologic reactions.

Because of the potential for cross-sensitivity between penicillamine and penicillin, monitor for allergic reaction in patients with a history of penicillin allergy.

Notify prescriber if patient reports decreased sense of taste, especially for salty and sweet Expect normal taste sensation to be restored (except in patients with Wilson’s disease) by giving of 5 to 10 mg of copper a day, as prescribed.

Monitor patients with diabetes mellitus for reduced insulin requirements to prevent risk of nighttime hypoglycemia because penicillamine may promote formation of anti-insulin antibodies.

Check liver function tests, as ordered, every 6 months (every 3 months for first year if patient has Wilson’s disease) during penacillamine therapy because drug may cause serious hepatic dysfunction.

PATIENT SAFTY

Advise patient to take penicillamine on an empty stomach.

Instruct men and nonpregnant women with cystinuria to increase fluid intake and follow prescribed low-methionine diet to minimize cystine production and enhance drug’s effectiveness. Urge patient to drink about 1 pint of fluid at bedtime and again during the night because this is when urine is more concentrated.

Tell patient to notify prescriber immediately if he develops a fever, sore throat, chills, bruising, or bleeding because drug may need to be stopped.

Instruct patient being treated for Wilson’s disease to follow a diet low in copper, avoiding such as broccoli, chocolate, copper-enriched cereals, liver, molasses, mushrooms, nuts, and shellfish. Inform her that it may take 1 to 3 months of therapy for her condition to improve.

Advise patient to consult prescriber before having dental work done during penicillamine therapy because drug can promote mouth ulcers.

Instruct patient to avoid consuming iron during penicillamine therapy because iron can decrease drug’s effectiveness.

Explain that sense of taste may decrease during penicillamine therapy. Advise patient to notify prescriber if it becomes intolerable.

Inform patient with rheumatoid arthritis that improvement may take 2 to 3 months of therapy.

Caution female patient to notify prescriber immediately if she becomes or may be pregnant because dosage may need to be reduced to prevent serious birth defects.

Category

Chemical class: Penicillin
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat systemic infections caused by gram-positive organisms (including Bacillus anthracis, Corynebacterium diphtheriae, enterococci, Listeria monocytogenes, Staphylococcus aureus, and S. epidermidis), gram-negative organisms (including Neisseria gonorrhoeae, N. meningitidis, Pasteurella multocida, and Streptobacillus moniliformis [ratbite fever]), and gram-positive anaerobes (including Actinomyces israelii [actinomycosis], Clostridium perfringens, C. tetani, Peptococcus species, Peptostreptococcus species, and spirochetes, especially Treponema carateum [pinta], T. pallidum, and T. pertenue [yaws])

ORALL

,(PENICILLIN G POTASSIUM) Adults and adolescents. 200,000 to 500,000 units (125 to 312 mg) every 4 to 6 hr. Maximum: 2 million units daily. Children. 4,167 to 15,000 units/kg every 4 hr, 6,250 to 22,500 units/kg every 6 hr, or 8,333 to 30,000 units/kg every 8 hr. (PENICILLIN V POTASSIUM) Adults and adolescents. 200,000 to 800,000 units (125 to 500 mg) every 6 to 8 hr. Maximum: 11,520,000 units (7,200 mg) daily Children. 4,167 to 13,280 units (2.5 to 8.3 mg)/kg every 4 hr, 6,250 to 20,000 units (3.75 to 12.5 mg)/kg every 6 hr, or 8,333 to 26,720 units (5 to 16.7 mg)/kg every 8 hr.

IV

,

IM

(PENICILLIN G POTASSIUM, PENICILLIN G SODIUM) Adults and adolescents. 1 to 5 million units every 4 to 6 hr. Maximum: 80 million units daily. Children. 8,333 to 16,667 units/kg every 4 hr or 12,500 to 25,000 units/kg every 6 hr. Premature and full-term neonates. 30,000 units/kg every 12 hr.
I.M.INJECTION(PENICILLIN G PROCAINE) Adults and adolescents. 600,000 to 1,200,000 units daily in divided doses every 12 to 24 hr. To treat moderately severe to severe streptococcal infections
I.M.INJECTION(PENICILLIN G BENZATHINE) Adults and children weighing more than 45 kg (100 lb). 1.2 million units as a single injection. Children weighing 27 to 45 kg (59 to 100 lb).900,000 units as a single injection. Children weighing less than 27 kg. 300,000 to 600,000 units as single injection. To treat congenital syphilis
I.M.INJECTION(PENICILLIN G BENZATHINE: BICILLIN L-A ONLY) Children under age 2. 50,000 units/kg as a single injection. To treat syphilis of less than 1 year’s duration
I.M.INJECTION(PENICILLIN G BENZATHINE: BICILLIN L-A ONLY) Adults and adolescents. 2.4 million units as a single injection. Children. 50,000 units/kg up to adult dosage as a single injection. Maximum: 2.4 million units/dose. To treat syphilis of more than 1 year’s duration
I.M.INJECTION(PENICILLIN G BENZATHINE: BICILLIN L-A ONLY) Adults and adolescents. 2.4 million units every wk for 3 wk. Children. 50,000 units/kg every wk for 3 wk. To treat bacterial meningitis

IV

,

IM

(PENICILLIN G POTASSIUM)
Adults. 50,000 units/kg every 4 hr or 24 million units daily in divided doses every 2 to 4 hr.

Mechanism of Action

Inhibits final stage of bacterial cell wall synthesis by competitively binding to penicillin-binding proteins inside the cell wall. Penicillin-binding proteins are responsible for various steps in bacterial cell wall synthesis. By binding to these proteins, penicillin leads to cell wall lysis.

Incompatibilities

Don’t mix any penicillin in the same syringe or container with aminoglycosides because aminoglycosides will be inactivated. Don’t mix penicillin G with that may result in a pH below 5.5 or above 8.

Contraindications

Hypersensitivity to penicillin or its components

Interactions

ACE inhibitors, potassium-containing , potassium-sparing diuretics: Increased risk of hyperkalemia (penicillin G potassium) chloramphenicol, erythromycin, sulfonamides, tetracycline, thrombolytics: Possibly interference with penicillin’s bactericidal effect cholestyramine, colestipol: Possibly impaired absorption of oral penicillin G methotrexate: Decreased methotrexate clearance, increased risk of toxicity oral contraceptives: Decreased contraceptive effectiveness (with penicillin V) probenecid: Increased blood penicillin level acidic beverages, such as fruit juices: Possibly altered effects of oral penicillin G

Side Efect

CNS: Confusion, dizziness, dysphasia, hallucinations, headache, lethargy, sciatic nerve irritation, seizures
CV: Labile blood pressure, palpitations
EENT: Black “hairy”tongue, oral candidiasis, stomatitis, taste perversion
GI: Abdominal pain, diarrhea, elevated liver function test results (transient), indigestion, nausea, pseudomembranous colitis
GU: Interstitial nephritis (acute), vaginal candidiasis
MS: Muscle twitching
SKIN: Rash
Other: Electrolyte imbalances; injection site necrosis, pain, or redness

Cautions

Obtain body tissue and fluid samples for culture and sensitivity tests as ordered before giving first dose. Expect to begin drug therapy before test results are known.

Reconstitute vials of penicillin for injection with sterile water for injection, D5W, or sodium chloride for injection.

Administer penicillin at least 1 hour before other antibiotics.

Inject I.M. form deep into large muscle mass. Apply ice to relieve pain.
WARNING Give penicillin G benzathine and penicillin G procaine only by deep I.M. injection; I.V. injection may be fatal, and intra-arterial injection may cause extensive tissue and organ necrosis.

Be aware that I.M. drug is absorbed slowly, which may make allergic reactions difficult to treat.

Assess patient for signs of secondary infection, such as profuse, watery diarrhea. If such diarrhea develops, contact prescriber and expect to obtain a stool specimen to rule out pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold pencillin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Monitor serum sodium level and assess for early signs of heart failure in patients receiving high doses of penicillin G sodium.

When giving penicillin G potassium to patient at risk for hypertension or fluid overload, be aware that each gram of pencillin G potassium also contains 1.02 mEq of sodium.

PATIENT SAFTY

Instruct patient to report previous allergies to penicillins and to notify prescriber immediately about

Side Efect

, including fever.

Advise patient who uses oral contraceptives to use an additional form of contraception during penicillin V therapy.

Urge patient to tell prescriber if diarrhea develops, even 2 months or more after penicillin therapy ends.

Category

Chemical class: Diamidine derivative
Therapeutic class: Antiprotozoal

Pregnancy category: C

Indications

To prevent Pneumocystis jiroveci (carinii) pneumonia ORAL INHALATION(NEBUPENT, PENTACARINAT) Adults and adolescents. 300 mg every 4 wk or 150 mg every 2 wk, using nebulizer and continuing until chamber is empty (30 to 45 min). ORAL INHALATION(PNEUMOPENT) Adults and adolescents. Initial: 60 mg every 24 to 72 hr for 5 doses over 2 wk, using ultrasonic nebulizer and continuing until nebulizer chamber is empty (about 15 min). Maintenance: 60 mg every 2 wk, using ultrasonic nebulizer and continuing until nebulizer chamber is empty. To treat P. jiroveci (carinii) pneumonia

IV

,

IM

Adults and children. 4 mg/kg daily for 14 to 21 days, given deep I.M. or by I.V. infusion over 1 to 2 hr.
DOSAGE ADJUSTMENT Dosage possibly reduced or I.V. infusion time or dosing interval extended for patients with renal failure.

Mechanism of Action

May bind to DNA and inhibit DNA replication in Pneumocystis jiroveci (carinii). Pentamidine also may inhibit dihydrofolate reductase, an enzyme needed to convert dihydrofolic acid to tetrahydrofolic acid in this organism. This action inhibits formation of coenzymes essential to growth and replication of P. jiroveci.

Incompatibilities

Don’t mix pentamidine with other or with saline solutions because precipitation may occur.

Contraindications

History of anaphylactic reaction to pentamidine or its components (inhalation form)

Interactions

bone marrow depressants, that cause blood dyscrasias: Increased risk of adverse hematologic effects didanosine: Increased risk of pancreatitis erythromycin (I.V.): Increased risk of torsades de pointes foscarnet: Increased risk of severe but reversible hypocalcemia, hypomagnesemia, and nephrotoxicity nephrotoxic : Increased risk of nephrotoxicity

Side Efect

CNS: Chills, confusion, dizziness, fatigue, fever, hallucinations, headache (I.V., I.M. forms)
CV: Arrhythmias, edema, hypotension, prolonged QT interval, torsades de pointes, ventricular tachycardia (I.V., I.M. forms)
EENT: Bitter or metallic taste (all forms), pharyngitis (inhalation form)
ENDO: Diabetes mellitus, hyperglycemia (I.V., I.M. forms); hypoglycemia (all forms)
GI: Abdominal pain, anorexia, diarrhea, elevated liver function test results, nausea, vomiting (I.V., I.M. forms); pancreatitis (all forms)
GU: Elevated serum creatinine level (I.V., I.M. forms); renal insufficiency (inhalation form)
HEME: Anemia, leukopenia, thrombocytopenia, unusual bleeding or bruising (I.V., I.M. forms)
MS: Myalgia (I.V., I.M. forms)
RESP: Bronchospasm, chest pain or congestion, cough, dyspnea, extrapulmonary pneumocystosis, pneumothorax (inhalation form)
SKIN: Night sweats (I.V., I.M. forms); rash (all forms)
Other: Hyperchloremic acidosis; hyperkalemia; hypocalcemia; hypomagnesemia; infusion site sterile abscess (I.V. form); injection site induration, pain, and phlebitis (I.M. form)

Cautions

Store pentamidine at room temperature, protected from light. Use within 24 hours after reconstitution.

For I.V. use, dissolve contents of 300-mg vial with 3 to 5 ml sterile water for injection or D5W. Further dilute in 50 to 250 ml D5W and infuse over 1 to 2 hours.

For I.M. use, dissolve contents of vial in 3 ml sterile water for injection and inject deep into large muscle mass. Be aware that I.M. administration increases risk of sterile abscess formation at injection site.

When giving drug I.V. or I.M., keep patient supine and monitor blood pressure frequently during and after administration. Keep emergency resuscitation equipment readily available.

Assess for hypoglycemia and arrhythmias in patient receiving I.V. or I.M. pentamidine. Although uncommon, these adverse reactions can be severe.

For inhalation, reconstitute contents of vial with 6 ml sterile water for injection (NebuPent or Pentacarinat) or 3 to 5 ml sterile water for injection or inhalation (Pneumopent). Reconstitute immediately before use. Don’t use normal saline solution because it causes precipitation. Place reconstituted drug in Respirgard II nebulizer, and set flow rate at 5 to 7 L/min for NebuPent or Pentacarinat. Don’t mix with other . For Pneumopent, place reconstituted drug in Fisoneb ultrasonic nebulizer and set flow rate at mid-flow mark.

Administer aerosolized pentamidine with patient in supine or recumbent position for best distribution of drug.

If patient who uses inhalation form has a history of asthma or smoking, notify prescriber if bronchospasm or a cough develops. She may need an aerosolized bronchodilator before each dose of pentamidine.

Monitor CBC; platelet count; liver function test results; BUN, serum creatinine and calcium, and blood glucose levels; and ECG tracing throughout therapy, as ordered.

Monitor blood glucose level because pentamidine use can induce insulin release from pancreas and severe hypoglycemia that can last from 1 day to several weeks.

Be aware that hyperglycemia and diabetes mellitus can occur up to several months after parenteral therapy stops.

PATIENT SAFTY

Stress importance of complying with prescribed administration schedule when pentamidine is used to prevent P. jiroveci (carinii) pneumonia.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to notify prescriber about unusual bleeding or bruising and to take precautions to avoid bleeding, as by using a soft-bristled toothbrush and an electric shaver.

Caution patient about possible hypoglycemic effects of pentamidine therapy.

Advise patient to have follow-up laboratory studies to test for diabetes mellitus, which can occur up to several months after stopping pentamidine therapy.

Category

Chemical class: Synthetic opioid
Therapeutic class: Analgesic

Pregnancy category: C

Controlled substance schedule: IV

Indications

To relieve moderate to severe pain I.V., I.M., OR SUBCUTANEOUS INJECTION
Adults. Initial: 30 mg every 3 to 4 hr, p.r.n. Maximum: 30 mg/single dose I.V., 60 mg/ single dose I.M. or subcutaneously, or 360 mg/24 hr for all parenteral forms. To relieve obstetric pain I.V. INJECTION
Adults. 20 mg when contractions become regular; repeated 2 or 3 times every 2 to 3 hr, as prescribed.
I.M.INJECTION
Adults. 30 mg as a single dose. Route Onset Peak Duration I.V. 2–3 min 15–30 min 2–3 hr I.M., 15–20 30–60 min 2–3 hr SubQ min

Mechanism of Action

Binds with opioid receptors, mainly kappa and sigma receptors, at many CNS sites to alter perception of and emotional response to pain.

Incompatibilities

Don’t mix pentazocine in same syringe with a soluble barbiturate because precipitation will occur.

Contraindications

Hypersensitivity to pentazocine or its components

Interactions

anticholinergics: Increased risk of urine retention and severe constipation antidiarrheals, antiperistaltics: Increased risk of severe constipation and CNS depression antihypertensives, diuretics, other hypotensionproducing : Additive hypotensive effects buprenorphine: Decreased pentazocine effectiveness, increased respiratory depression
CNS depressants: Increased CNS depression, increased risk of habituation hydroxyzine, other opioid analgesics: Increased analgesia, CNS depression, and hypotensive effects
MAO inhibitors: Increased risk of unpredictable, severe, even fatal

Side Efect

metoclopramide: Antagonized metoclopramide effects on GI motility naloxone: Antagonized analgesic, CNS, and respiratory depressant effects of pentazocine
naltrexone: Withdrawal symptoms in patients physically dependent on pentazocine neuromuscular blockers: Increased respiratory depression
alcohol use: Additive CNS depression and increased risk of habituation

Side Efect

CNS: Chills, dizziness, drowsiness, euphoria, fatigue, headache, insomnia, light-headedness, nervousness, nightmares, paresthesia, restlessness, weakness
CV: Hypotension, tachycardia
EENT: Blurred vision, diplopia, dry mouth, laryngeal edema, laryngospasm
GI: Constipation, hepatotoxicity, nausea, vomiting
GU: Decreased urine output, dysuria, urinary frequency, urine retention
MS: Muscle rigidity (with large doses)
RESP: Atelectasis, bronchospasm, dyspnea, hypoventilation, wheezing
SKIN: Diaphoresis, erythema multiforme, facial flushing, pruritus, rash, StevensJohnson syndrome, toxic epidermal necrolysis, urticaria
Other: Facial edema; injection site burning, pain, redness, or swelling; physical and psychological dependence

Cautions

Use pentazocine with extreme caution in patients with head injury, intracranial lesion, or increased intracranial pressure. Drug may mask neurologic evidence.

Use pentazocine cautiously in patients physically dependent on opioid agonists because drug may prompt withdrawal symptoms; in patients with acute MI because drug’s cardiovascular effects can increase cardiac workload; in patients with renal or hepatic dysfunction because drug is metabolized in liver and excreted in urine; and in patients with respiratory conditions because drug depresses respiratory system.

When giving repeated parenteral doses, use I.M. or I.V. route when possible and as prescribed because subcutaneous route may cause severe tissue damage at injection site. Rotate I.M. sites to avoid tissue damage.

After giving parenteral form, expect to taper dosage gradually, as prescribed, to reduce the risk of withdrawal symptoms.

PATIENT SAFTY

Caution patient that prolonged use of pentazocine may result in dependence.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Caution patient not to use alcohol or OTC without consulting prescriber.

Advise patient to report possible allergic reaction, such as a rash or itching.

Category

Chemical class: Barbiturate
Therapeutic class: Anticonvulsant, sedativehypnotic

Pregnancy category: D

Controlled substance schedule: II (oral, parenteral), III (rectal)

Indications

To provide daytime sedation ELIXIR
Adults. 20 mg t.i.d. or q.i.d. Children. 2 to 6 mg/kg daily. SUPPOSITORIES
Adults. 30 mg b.i.d. to q.i.d. Children. 2 mg/kg t.i.d. To provide short-term treatment of insomnia , ELIXIR
Adults. 100 mg at bedtime. I.V. INJECTION
Adults. Initial: 100 mg, with additional small doses at 1-min intervals, as prescribed. Maximum: 500 mg.
I.M.INJECTION
Adults. 150 to 200 mg at bedtime. SUPPOSITORIES Adults and adolescents over age 14. 120 to 200 mg at bedtime. Children ages 12 to 14. 60 to 120 mg at bedtime. Children ages 5 to 12. 60 mg at bedtime. Children ages 1 to 4. 30 to 60 mg at bedtime. Infants ages 2 months to 1 year.30 mg at bedtime. To provide preoperative sedation , ELIXIR
Adults. 100 mg before surgery. Children. 2 to 6 mg/kg before surgery. Maximum: 100 mg/dose.
I.M.INJECTION
Adults. 150 to 200 mg before surgery. Children. 2 to 6 mg/kg before surgery. Maximum: 100 mg/dose. SUPPOSITORIES Children ages 12 to 14. 60 to 120 mg before surgery. Children ages 5 to 12. 60 mg before surgery. Children ages 1 to 4. 30 to 60 mg before surgery. Infants ages 2 months to 1 year. 30 mg before surgery. To provide emergency treatment of seizures associated with eclampsia, meningitis, status epilepticus, tetanus, or toxic reactions to local anesthetics or strychnine I.V. INJECTION
Adults. 100 mg, with additional small doses at 1-min intervals, as prescribed. Maximum: 500 mg. Children. 50 mg, with additional small doses at 1-min intervals, as prescribed, until desired effect occurs.
I.M.INJECTION Children. 50 mg, with additional small doses at 1-min intervals, as prescribed, until desired effect occurs.
DOSAGE ADJUSTMENT Dosage possibly reduced for elderly or debilitated patients and those with hepatic dysfunction. Route Onset Peak Duration P.O., P.R. 15–60 min 1–4 hr 3–4 hr I.V. In 1 min Unknown 15 min I.M. 10–25 min Unknown 3–4 hr

Mechanism of Action

Inhibits ascending conduction in reticular formation, which controls CNS arousal to produce drowsiness, hypnosis, and sedation. Pentobarbital also decreases spread of seizure activity in cortex, thalamus, and limbic system. It promotes an increased threshold for electrical stimulation in the motor cortex, which may contribute to anticonvulsant effects.

Contraindications

Hepatic disease; history of addiction to hypnotics or sedatives; hypersensitivity to pentobarbital, barbiturates, or their components; nephritis; porphyria; severe respiratory disease with airway obstruction or dyspnea

Interactions

acetaminophen: Possibly decreased effects of acetaminophen (long-term pentobarbital use) carbamazepine, chloramphenicol, corticosteroids, cyclosporine, dacarbazine, digoxin, disopyramide, doxycycline, griseofulvin, metronidazole, oral contraceptives, phenylbutazone, quinidine, theophyllines,
vitamin D: Decreased effectiveness of these
CNS depressants: Increased CNS depression and risk of habituation divalproex sodium,
valproic acid: Increased risk of CNS toxicity and neurotoxicity guanadrel, guanethidine: Possibly increased risk of orthostatic hypotension halogenated hydrocarbon anesthetic: Increased risk of hepatotoxicity (with longterm pentobarbital use)
haloperidol: Possibly decreased blood haloperidol level, possibly altered seizure pattern or frequency hydantoins: Possibly interference with hydantoin metabolism leucovorin: Possibly decreased anticonvulsant effect of pentobarbital maprotiline: Possibly enhanced CNS depression and decreased therapeutic effects of pentobarbital
mexiletine: Possibly decreased blood mexiletine level oral anticoagulants: Possibly decreased effects of these , possibly increased risk of bleeding when pentobarbital stops tricyclic antidepressants: Possibly decreased therapeutic effects of these
alcohol use: Increased CNS depression

Side Efect

CNS: Agitation, anxiety, ataxia, confusion, delusions, depression, dizziness, drowsiness, fever, hallucinations, headache, insomnia, irritability, nervousness, nightmares, paradoxical stimulation, seizures, syncope, tremor
CV: Orthostatic hypotension
EENT: Vision changes
GI: Anorexia, constipation, hepatic dysfunction, nausea, vomiting
HEME: Agranulocytosis
MS: Arthralgia, bone pain, muscle twitching or weakness
RESP: Respiratory depression
SKIN: Exfoliative dermatitis, rash, StevensJohnson syndrome
Other: Physical and psychological dependence, weight loss

Cautions

Use pentobarbital with extreme caution in patients with depression, a history of drug abuse, or suicidal tendencies.

Use drug cautiously in elderly or debilitated patients and those with acute or chronic pain because it may induce paradoxical stimulation.

When using I.V. route, inject drug at 50 mg/min or less to avoid adverse respiratory and circulatory reactions.

If patient shows premonitory signs of hepatic coma, withhold drug and notify prescriber immediately.

Monitor I.V. site closely and avoid extravasation. Drug is highly alkaline and may cause local tissue damage and necrosis.

PATIENT SAFTY

Inform patient that pentobarbital is habitforming, and stress the importance of taking it exactly as prescribed.

Instruct patient who takes elixir form to use a calibrated measuring device and to close container tightly after use.

Instruct patient who uses suppositories to refrigerate them.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Urge patient to avoid alcohol and other CNS depressants because they may increase drug’s adverse CNS effects.

Category

Chemical class: Low-molecular-weight heparin-like compound
Therapeutic class: Local anti-inflammatory (bladder-specific)

Pregnancy category: B

Indications

To relieve bladder discomfort or pain caused by interstitial cystitis
Adults. 100 mg t.i.d. for up to 3 mo, possibly followed by another 3 mo if no improvement and no

Side Efect

.

Mechanism of Action

Adheres to mucosal membrane of bladder wall and may block irritating solutes from reaching cells, thereby decreasing local pain and discomfort.

Contraindications

Hypersensitivity to pentosan, other structurally related compounds, or their components

Interactions

alteplase (recombinant), aspirin (high doses), heparin, oral anticoagulants, streptokinase: Increased risk of hemorrhage

Side Efect

CNS: Depression, dizziness, emotional lability, headache
GI: Abdominal pain, diarrhea, elevated liver enzyme levels, hepatic dysfunction, indigestion, nausea, rectal hemorrhage
HEME: Unusual bleeding or bruising
SKIN: Alopecia, rash

Cautions

Use pentosan with extreme caution in patients with conditions that increase bleeding risk, such as aneurysm, diverticula, GI ulceration, hemophilia, polyps, and thrombocytopenia (especially heparininduced).

Use drug cautiously in patients with hepatic dysfunction because drug is desulfated in liver and spleen.

Monitor patient for abnormal bleeding, such as unexplained bruises and epistaxis, because drug is a weak anticoagulant.

PATIENT SAFTY

Instruct patient to take pentosan with a full glass of water at least 1 hour before or 2 hours after meals.

Explain the pattern of exacerbations and remissions with interstitial cystitis. Reassure patient that symptoms should improve within 3 months after starting pentosan therapy.

Advise patient to take bleeding precautions during therapy, such as using an electric shaver and a soft-bristled toothbrush.

If alopecia develops, explain that it’s usually confined to a single area.

Category

Chemical class: Xanthine derivative
Therapeutic class: Blood viscosity reducer

Pregnancy category: C

Indications

To treat peripheral vascular disease
Adults. 400 mg t.i.d. with meals.
DOSAGE ADJUSTMENT Dosage possibly reduced to 400 mg b.i.d. for patients who experience adverse GI or CNS reactions. Route Onset Peak Duration P.O. 2–4 wk Unknown Unknown

Mechanism of Action

Relieves symptoms of peripheral vascular disease by:

reducing blood viscosity by decreasing plasma fibrinogen level and inhibiting RBC and platelet aggregation

improving erythrocyte flexibility by inhibiting phosphodiesterase and increasing the amount of cAMP in RBCs

decreasing peripheral vascular resistance and improving microcirculatory blood flow and tissue oxygenation.

Contraindications

Hypersensitivity to pentoxifylline, methylxanthines (such as caffeine, theophylline, and theobromine), or their components; recent cerebral or retinal hemorrhage

Interactions

antihypertensives: Potentiated antihypertensive effects cefamandole, cefoperazone, cefotetan, heparin, oral anticoagulants, other platelet aggregation inhibitors, plicamycin, thrombolytics,
valproic acid: Increased risk of bleeding
cimetidine: Increased blood pentoxifylline level, increased risk of adverse effects sympathomimetics, xanthines: Enhanced CNS stimulation smoking: Possibly decreased therapeutic effects of pentoxifylline

Side Efect

CNS: Asceptic meningitis, dizziness, headache
GI: Indigestion, nausea, vomiting

Cautions

Use pentoxifylline cautiously in elderly patients and those with hepatic or renal dysfunction.

Give drug with meals and an antacid, if needed, to reduce adverse GI reactions.

PATIENT SAFTY

Instruct patient to swallow pentoxifylline tablets whole and not to crush, break, or chew them.

Advise patient to take drug with meals to reduce GI irritation. If adverse GI reactions occur anyway, advise her to also take an antacid with meals.

Although symptoms may not improve for several weeks, urge patient to continue taking drug as prescribed to achieve maximum therapeutic effect.

Instruct patient not to smoke during therapy because smoking constricts blood vessels and may reduce drug effectiveness.

Urge patient to report

Side Efect

; dosage may need reduction.

Category

Chemical class: Perindoprilat prodrug
Therapeutic class: Antihypertensive

Pregnancy category: D

Indications

To manage hypertension
Adults. Initial: 4 mg daily as a single dose or in divided doses b.i.d., increased as prescribed until blood pressure is controlled or maximum dosage is reached. Maintenance: 4 to 8 mg daily. Maximum: 8 mg daily.
DOSAGE ADJUSTMENT If patient takes a diuretic, initial dosage possibly reduced to 2 to 4 mg daily; if patient has renal failure, initial dosage possibly reduced to 2 mg daily. To reduce risk of cardiovascular death or nonfatal MI in patients with stable coronary artery disease
Adults. Initial: 4 mg daily for 2 wk; then increased to 8 mg daily. Maintenance: 8 mg daily.
DOSAGE ADJUSTMENT If patient is elderly, 2 mg daily for 1 wk, increased to 4 mg daily for 1 wk and then to 8 mg daily if tolerated.

Mechanism of Action

Is converted to the active metabolite perindoprilat, which competes with angiotensin I binding sites, blocking conversion of angiotensin I to angiotensin II, a potent vasoconstrictor. As a result, this ACE inhibitor reduces vasoconstriction and blood pressure. Decreased angiotensin II also reduces aldosterone secretion, increasing renal excretion of water and sodium.

Contraindications

History of angioedema with ACE inhibitor treatment; hypersensitivity to perindopril, other ACE inhibitors, or their components

Interactions

diuretics: Increased risk of hypotension lithium: Increased blood lithium level and risk of toxicity potassium-sparing diuretics, potassium supplements: Increased risk of hyperkalemia sodium aurothiomalate: Increased risk of nitritoid reaction with facial flushing, nausea, vomiting, and hypotension

Side Efect

CNS: Amnesia, anxiety, dizziness, fatigue, fever, headache, hypertonia, migraine, syncope, vertigo
CV: Chest pain, ECG changes, heart murmur, hypotension, orthostatic hypotension, palpitations, PVCs
EENT: Conjunctivitis, earache, epistaxis, hoarseness, pharyngitis, rhinitis, sinusitis, sneezing, tinnitus
GI: Abdominal pain, diarrhea, elevated liver function test results, flatulence, increased appetite, indigestion
GU: Flank pain, renal calculi, urinary frequency and urgency, vaginitis
HEME: Hematoma, leukopenia, neutropenia
MS: Arthritis, back pain, gout, limb pain, myalgia, neck pain
RESP: Cough
SKIN: Canker sores, diaphoresis, dry skin, ecchymosis, erythema, pruritus, rash
Other: Angioedema, facial edema

Cautions

Use cautiously with heart failure, renal artery stenosis, or renal dysfunction.

Also use cautiously in elderly patients, and watch closely for adverse effects such as dizziness or vertigo, because these patients have an increased risk of falling.

Monitor patients with hepatic dysfunction for enhanced therapeutic drug effects because drug’s bioavailability is increased.

Monitor serum potassium level to detect hyperkalemia, especially in patients with renal insufficiency or diabetes mellitus and those who use a potassium-containing salt substitute or take a potassium-sparing diuretic or potassium supplement.

PATIENT SAFTY

Instruct patient to take perindopril exactly as prescribed, even if she feels well.
WARNING Urge patient to stop taking drug and notify prescriber immediately if she experiences signs of angioedema.

Advise patient to notify prescriber at once about fever, sore throat, or other signs that may indicate neutropenia.

Urge patient to avoid potassium supplements and potassium-containing salt substitutes unless prescriber approves.

Instruct patient to avoid hazardous activities until drug’s CNS effects are known.

Advise woman to promptly report suspected, known, or intended pregnancy. Drug will need to be discontinued.

Category

Chemical class: Piperazine phenothiazine
Therapeutic class: Antiemetic, antipyschotic

Pregnancy category: Not rated

Indications

To treat psychotic disorders

ORALL

Hospitalized adults and adolescents.8 to 16 mg b.i.d. to q.i.d., adjusted as prescribed and tolerated. Maximum: 64 mg daily. Adults and adolescents. 4 to 16 mg b.i.d. to q.i.d., adjusted as prescribed and tolerated. Maximum: 64 mg daily.
I.M.INJECTION Adults and adolescents. 5 to 10 mg every 6 hr, adjusted as prescribed and tolerated. Maximum: 15 mg daily for outpatients, 30 mg daily for hospitalized patients. To treat severe nausea and vomiting Adults and adolescents. 8 to 16 mg daily in divided doses, decreased as appropriate. Maximum: 24 mg daily.

IV

OR INJECTION Adults and adolescents. 1 mg every 1 to 2 min, up to 5 mg total.
I.M.INJECTION Adults and adolescents. 5 mg, increased to 10 mg as ordered for rapid control of severe vomiting. Maximum: 15 mg daily for outpatients, 30 mg daily for hospitalized patients.
DOSAGE ADJUSTMENT Initial dose possibly reduced and gradually increased for elderly, emaciated, or debilitated patients. Adolescents may need low adult dosage. Route Onset Peak Duration P.O. Several wk 4–7 days Unknown I.M. Unknown 1–2 hr 6 hr

Mechanism of Action

Depresses areas of the brain that control activity and aggression, including cerebral cortex, hypothalamus, and limbic system, by an unknown mechanism. Perphenazine also prevents nausea and vomiting by inhibiting or blocking dopamine receptors in medullary chemoreceptor trigger zone and peripherally by blocking vagus nerve in the GI tract.

Incompatibilities

Don’t mix perphenazine oral solution with beverages that contain caffeine or tannins (such as coffee, colas, and teas) or pectinates (such as apple juice) because they’re physically incompatible.

Contraindications

Blood dyscrasias; bone marrow depression; cerebral arteriosclerosis; coma; concurrent use of CNS depressants (large doses); coronary artery disease; hepatic impairment; hypersensitivity to perphenazine, other phenothiazines, or their components; myeloproliferative disorders; severe CNS depression; severe hypertension or hypotension; subcortical brain damage

Interactions

aluminumand magnesium-containing antacids, antidiarrheals (adsorbent): Decreased absorption of oral perphenazine amantadine, anticholinergics, antidyskinetics, antihistamines: Increased adverse anticholinergic effects amphetamines: Decreased therapeutic effects of both anticonvulsants: Decreased seizure threshold, inhibited metabolism and toxicity of anticonvulsant antithyroid : Increased risk of agranulocytosis apomorphine: Additive CNS depression, decreased emetic response to apomorphine if perphenazine is given first appetite suppressants (except phenmetrazine): Antagonized anorectic effect of appetite suppressants
beta blockers: Increased blood levels of both and risk of arrhythmias, hypotension, irreversible retinopathy, and tardive dyskinesia bromocriptine: Possibly interference with bromocriptine’s effects
CNS depressants: Increased CNS and respiratory depression and hypotensive effects dopamine: Antagonized peripheral vasoconstriction with high doses of dopamine ephedrine: Decreased vasopressor response to ephedrine epinephrine: Blocked alpha-adrenergic effects of epinephrine, possibly causing severe hypotension and tachycardia hepatotoxic : Increased risk of hepatotoxicity hypotension-causing : Increased risk of severe orthostatic hypotension levodopa: Inhibited antidyskinetic effects of levodopa lithium: Possibly neurotoxicity (disorientation, extrapyramidal symptoms, unconsciousness) maprotiline, selective serotonin reuptake inhibitors, tricyclic antidepressants: Prolonged and intensified sedative and anticholinergic effects of these or perphenazine metrizamide: Decreased seizure threshold opioid analgesics: Increased CNS and respiratory depression, increased risk of orthostatic hypotension and severe constipation ototoxic , especially antibiotics: Possibly masking of some symptoms of ototoxicity, such as dizziness, tinnitus, and vertigo probucol, other that prolong QT interval: Prolonged QT interval, which may increase risk of ventricular tachycardia thiazide diuretics: Possibly hyponatremia and water intoxication
alcohol use: Increased CNS and respiratory depression, hypotensive effects, and risk of heatstroke

Side Efect

CNS: Behavioral changes, cerebral edema, dizziness, drowsiness, extrapyramidal reactions (such as akathisia, dystonia, pseudoparkinsonism), fever, headache, neuroleptic malignant syndrome, seizures, suicidal ideation, syncope, tardive dyskinesia (persistent)
CV: Bradycardia, cardiac arrest, hypertension, hypotension, orthostatic hypotension, tachycardia
EENT: Blurred vision, dry mouth, glaucoma, laryngeal edema, miosis, mydriasis, nasal congestion, ocular changes (corneal opacification, retinopathy)
ENDO: Decreased libido, galactorrhea, gynecomastia, syndrome of inappropriate ADH secretion
GI: Anorexia, constipation, diarrhea, fecal impaction, nausea, vomiting
GU: Bladder paralysis, ejaculation failure, menstrual irregularities, polyuria, urinary frequency, urinary incontinence, urine retention
HEME: Agranulocytosis, eosinophilia, hemolytic anemia, leukopenia, pancytopenia, thrombocytopenic purpura
RESP: Asthma
SKIN: Diaphoresis, eczema, erythema, exfoliative dermatitis, hyperpigmentation, jaundice, pallor, photosensitivity, pruritus, urticaria
Other: Anaphylaxis, angioedema

Cautions

Perphenazine shouldn’t be used to treat dementia-related psychosis in the elderly because of an increased mortality risk.

Use perphenazine cautiously in patients with depression or hepatic, pulmonary, or renal dysfunction and in elderly patients, who are at increased risk for increased plasma concentrations and tardive dyskinesia.

For I.V. use, dilute drug to 0.5 mg/ml with sodium chloride for injection. Protect solution from light. Slight yellowing is acceptable, but discard solution if it’s markedly discolored or contains precipitate.

Obtain blood samples for CBC and liver and renal function tests, as ordered, to detect

Side Efect

.

Monitor temperature frequently, and notify prescriber if it rises; a significant increase suggests drug intolerance.

Monitor blood pressure of patient who takes large doses of perphenazine, especially if surgery is indicated, because of the increased risk of hypotension.

Watch patient closely (especially children, adolescents, and young adults), for suicidal tendencies, particularly when perphenazine therapy starts and dosage changes, because depression may worsen temporarily during these times, possibly leading to suicidal ideation.

PATIENT SAFTY

Instruct patient to take drug exactly as prescribed to ensure optimal effectiveness and minimize

Side Efect

.

Remind patient who takes oral solution to use a calibrated measuring device.

Instruct patient taking oral solution to dilute every 5 ml (teaspoon) of drug in 2 fluid oz of water, milk, tomato juice, fruit juice (except apple), soup, or carbonated beverage. Caution against using beverages that contain caffeine or tannins (cola, coffee, tea).

Caution patient not to spill oral solution on skin or clothing because it can cause contact dermatitis and damage clothing.

Urge patient to avoid alcohol and other CNS depressants during perphenazine therapy and to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to avoid excessive sun exposure and to protect skin when outdoors.

Instruct patient to notify prescriber about persistent or severe

Side Efect

.

Urge patient to comply with long-term follow-up to detect

Side Efect

and determine possible need for perphenazine
DOSAGE ADJUSTMENTs.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes and particularly if patient is a child, teenager, or young adult.

Category

Chemical class: Azo dye
Therapeutic class: Urinary analgesic

Pregnancy category: B

Indications

To relieve burning and pain on urination, and urinary frequency and urgency Adults and adolescents. 200 mg t.i.d. with or without food for no longer than 2 days. Children. 4 mg/kg t.i.d. with food for no longer than 2 days.

Mechanism of Action

Exerts a topical or local anesthetic effect on urinary tract mucosa as drug is excreted in urine. Phenazopyridine’s exact mechanism is unknown.

Contraindications

Hypersensitivity to phenazopyridine or its components, renal insufficiency

Side Efect

CNS: Headache
GI: Indigestion, nausea, vomiting
GU: Reddish orange urine
SKIN: Pruritus, rash
Other: Discoloration of body fluids

Cautions

Notify prescriber if yellowish skin or sclerae develop in patient taking phenazopyridine because this may indicate drug accuphenazopyridine hydrochloride 813 P mulation from impaired renal excretion. Expect prescriber to discontinue drug.

Be aware that phenazopyridine treatment should be limited to 2 days in patients with UTI.

PATIENT SAFTY

Instruct patient not to take drug for longer than 2 days and to notify prescriber if symptoms persist beyond that time.

If GI distress develops, advise patient to take drug with meals.

Inform patient that drug turns urine orange to red and may discolor other body fluids, such as tears.

Advise patient not to wear contact lenses during therapy because they may become stained.

Category

Chemical class: Hydrazine derivative
Therapeutic class: Antidepressant

Pregnancy category: C

Indications

To treat depression
Adults. Initial: 1 mg/kg daily, increased gradually as prescribed and tolerated. Maintenance: 45 mg daily. Maximum: 90 mg daily.
DOSAGE ADJUSTMENT For elderly patients, initially may be reduced to 0.8 to 1 mg/kg daily in divided doses, increased as ordered and tolerated to maximum of 60 mg daily. Route Onset Peak Duration P.O. 7–10 days 4–8 wk 10 days

Contraindications

Cardiovascular disease; cerebrovascular disease; heart failure; hepatic disease; history of headaches; hypersensitivity to phenelzine or its components; hypertension; pheochromocytoma; severe renal impairment; use of anesthetics, antihypertensives, bupropion, buspirone, carbamazepine, CNS depressants, cyclobenzaprine, dextromethorphan, meperidine, selective serotonin-reuptake inhibitors, sympathomimetics, or tricyclic antidepressants; use within 14 days of other MAO inhibitor

Interactions

anticholinergics, antidyskinetics, antihistamines: Increased anticholinergic effect, prolonged CNS depression (antihistamines) anticonvulsants: Increased CNS depression, possibly altered pattern of seizures
beta blockers: Increased risk of bradycardia bromocriptine: Possibly interference with bromocriptine effects
bupropion: Increased risk of bupropion toxicity buspirone: Increased risk of hypertension caffeine-containing : Increased risk of dangerous arrhythmias and severe hypertension carbamazepine, cyclobenzaprine, maprotiline, other
MAO inhibitors: Increased risk of hyperpyretic crisis, hypertensive crisis, severe seizures, and death; altered pattern of seizures (with carbamazepine)
CNS depressants: Increased CNS depression dextromethorphan: Increased risk of excitation, hypertension, and hyperpyrexia diuretics: Increased hypotensive effect doxapram: Increased vasopressor effects of either drug fluoxetine: Increased risk of agitation, confusion, GI symptoms, hyperpyretic episodes, hypertensive crisis, potentially fatal serotonin syndrome, restlessness, and severe seizures. guanadrel, guanethidine: Increased risk of hypertension haloperidol, loxapine, molindone, phenothiazines, pimozide,
thioxanthenes: Prolonged and intensified anticholinergic, hypotensive, and sedative effects of these or phenelzine insulin, oral antidiabetic : Increased hypoglycemic effects levodopa: Increased risk of sudden, moderate to severe hypertension local anesthetics (with epinephrine or levonordefrin): Possibly severe hypertension meperidine, other opioid analgesics: Increased risk of coma, hyperpyrexia, hypotension, immediate excitation, rigidity, seizures, severe hypertension, severe respiratory depression, sweating, vascular collapse, and death methyldopa: Increased risk of hallucinaphenelzine sulfate 814 tions, headache, hyperexcitability, and severe hypertension
methylphenidate: Increased CNS stimulant effect of methylphenidate metrizamide: Decreased seizure threshold, increased risk of seizures oral anticoagulants: Increased anticoagulant activity paroxetine, sertraline, trazodone, tricyclic antidepressants: Increased risk of potentially fatal serotonin syndrome phenylephrine (nasal or ophthalmic): Potentiated vasopressor effect of phenylephrine rauwolfia alkaloids: Increased risk of moderate to severe hypertension, CNS depression (when phenelzine is added to rauwolfia alkaloid therapy), CNS excitation and hypertension (when rauwolfia alkaloid is added to phenelzine therapy) spinal anesthetics: Increased risk of hypotension succinylcholine: Possibly increased neuromuscular blockade of succinylcholine sympathomimetics: Prolonged and intensified cardiac stimulant and vasopressor effects tryptophan: Increased risk of confusion, disorientation, hyperreflexia, hyperthermia, hyperventilation, mania or hypomania, and shivering and beverages high in tyramine or other pressor amines, such as aged cheese; beer; fava beans or other broad beans; cured meat or sausage; liqueurs; overripe fruit; red and white wine; reduced-alcohol and alcoholfree beer and wine; sauerkraut; sherry; smoked or pickled fish, meats, and poultry; yeast or protein extracts: Increased risk of sudden, severe hypertension
alcohol use: Increased CNS depressant effects and hypertensive crisis

Side Efect

CNS: Agitation, dizziness, drowsiness, headache, overstimulation, restlessness, sedation, sleep disturbance, suicidal ideation, weakness
CV: Bradycardia, edema, hypertensive crisis, orthostatic hypotension, palpitations, tachycardia
EENT: Blurred vision, dry mouth, photophobia
ENDO: Hypoglycemia in diabetic patients
GI: Abdominal pain, constipation, diarrhea, Serotonin production Postsynaptic cell Serotonin receptor Serotonin Phenelzine Monoamine nerve ending Serotonin production MAO MAO Serotonin production Postsynaptic cell Serotonin receptor Serotonin Phenelzine Monoamine nerve ending Serotonin production MAO MAO

Mechanism of Action

Phenelzine relieves symptoms of unipolar depressive disorders by inhibiting the enzyme monoamine oxidase (MAO). Normally, MAO breaks down monoamine neurotransmitters, such as serotonin, as shown below left. By inhibiting this enzyme, phenelzine increases the concentration of serotonin in the vesicles of monoamine nerve endings, allowing more serotonin to be released and engage with receptors on postsynaptic cells, as shown below right. A serotonin deficiency may be responsible in part for endogenous depression. elevated liver function test results, increased appetite, nausea
GU: Impotence, priapism, sexual dysfunction, urinary frequency, urine retention
MS: Muscle twitching
SKIN: Diaphoresis, rash
Other: Hypernatremia, weight gain

Cautions

Use phenelzine cautiously in patients with epilepsy because drug may alter seizure threshold.

Use phenelzine cautiously in patients with diabetes mellitus because insulin sensitivity may increase, predisposing patient to hypoglycemia.

Expect to observe some therapeutic effect within 7 to 10 days, but keep in mind that full effect may not occur for 4 to 8 weeks.

Monitor cardiovascular status closely for changes in heart rate (especially if patient receives more than 30 mg daily) and signs of life-threatening hypertensive crisis. Question patient often about headaches and palpitations. If either occurs, notify prescriber and expect to discontinue drug.

Keep phentolamine readily available to treat hypertensive crisis. Give 5 mg by slow I.V., as prescribed, to reduce blood pressure without causing excessive hypotension. Use external cooling measures, as prescribed, to manage fever.

To avoid hypertensive crisis, expect to wait 10 to 14 days, as prescribed, when switching patient from one MAO inhibitor to another or when switching from a dibenzazepine-related drug, such as amitriptyline or perphenazine.

Watch closely for suicidal tendencies, especially in children, adolescents, and young adults and especially when therapy starts or dosage changes.

PATIENT SAFTY

Inform patient and family members that therapeutic effects of phenelzine may take several weeks to appear and that she should continue taking drug as prescribed.

Caution patient to rise slowly from a lying or sitting position to minimize effects of orthostatic hypotension.
WARNING Instruct patient to avoid the following , beverages, and during phenelzine therapy and for 2 weeks afterward: alcohol-free and reduced-alcohol beer and wine; appetite suppressants; beer; broad beans; cheese (except cottage and cream cheese); chocolate and caffeine in large quantities; dry sausage (including Genoa salami, hard salami, pepperoni, and Lebanon bologna); hay fever ; inhaled asthma ; liver; meat extract; OTC cold and cough preparations (including those containing dextromethorphan), nasal decongestants (tablets, drops, or spray); pickled herring; products that contain tryptophan; protein-rich that may have undergone protein changes by aging, pickling, fermenting, or smoking; sauerkraut; sinus ; weight-loss preparations; yeast extracts (including brewer’s yeast in large quantities); yogurt; and wine.

Advise patient to inform all health care providers (including dentists) that she takes an MAO inhibitor because certain are contraindicated within 2 weeks.

Urge patient to avoid hazardous activities until drug’s CNS effects are known.

Stress the importance of reporting headaches and other unusual, persistent, or severe symptoms.

Tell family or caregiver to watch closely for suicidal tendencies, especially in children, adolescents, and young adults and especially when therapy starts or dosage changes.

Urge patient with diabetes who’s taking insulin or an oral antidiabetic to check blood glucose level often during therapy because phenelzine may affect glucose control.

Category

Chemical class: Barbiturate
Therapeutic class: Anticonvulsant, sedativehypnotic

Pregnancy category: D

Controlled substance schedule: IV

Indications

To treat seizures , ELIXIR,
Adults. 60 to 250 mg daily as a single dose or in divided doses. Children. 1 to 6 mg/kg daily as a single dose or in divided doses. I.V. INJECTION
Adults. 100 to 320 mg, repeated as needed and as prescribed. Maximum: 600 mg daily. Children. Initial: 10 to 20 mg/kg as a single dose. Maintenance: 1 to 6 mg/kg daily. To treat status epilepticus

IV

OR INJECTION
Adults. 10 to 20 mg/kg given slowly and repeated as needed and as prescribed. Children. 15 to 20 mg/kg over 10 to 15 min. To provide short-term treatment of insomnia , ELIXIR,
Adults. 100 to 320 mg at bedtime. I.V., I.M., OR SUBCUTANEOUS INJECTION
Adults. 100 to 325 mg at bedtime. To provide daytime sedation , ELIXIR,
Adults. 30 to 120 mg daily in divided doses b.i.d. or t.i.d. Children. 2 mg/kg t.i.d. I.V., I.M., OR SUBCUTANEOUS INJECTION
Adults. 30 to 120 mg daily in divided doses b.i.d. or t.i.d. To provide preoperative sedation , ELIXIR, Children. 1 to 3 mg/kg before surgery.
I.M.INJECTION
Adults. 130 to 200 mg 60 to 90 min before surgery. I.V. OR

IM

Children. 1 to 3 mg/kg 60 to 90 min before surgery.
DOSAGE ADJUSTMENT Dosage possibly reduced for elderly or debilitated patients to minimize confusion, depression, and excitement. Route Onset Peak Duration P.O. 20–60 min Unknown Unknown I.V. 5 min 30 min 4–6 hr I.M., 5–20 min Unknown 4–6 hr SubQ

Mechanism of Action

Inhibits ascending conduction of impulses in the reticular formation, which controls CNS arousal to produce drowsiness, hypnosis, and sedation. Phenobarbital also decreases the spread of seizure activity in cortex, thalamus, and limbic system. It promotes an increased threshold for electrical stimulation in the motor cortex, which may contribute to its anticonvulsant properties.

Contraindications

Hepatic disease; history of addiction to hypnotics or sedatives; hypersensitivity to phenobarbital, other barbiturates, or their components; nephritis; porphyria; severe respiratory disease with airway obstruction or dyspnea

Interactions

acetaminophen: Decreased acetaminophen effectiveness with long-term phenobarbital therapy amphetamines: Delayed intestinal absorption of phenobarbital anesthetics (halogenated hydrocarbon): Possibly hepatotoxicity anticonvulsants (hydantoin): Unpredictable effects on metabolism of anticonvulsant anticonvulsants (succinimide), including carbamazepine: Decreased blood levels and elimination half-lives of these calcium channel blockers: Possibly excessive hypotension carbonic anhydrase inhibitors: Enhanced osteopenia induced by phenobarbital chloramphenicol, corticosteroids, cyclosporine, dacarbazine, digoxin, metronidazole, quinidine: Decreased effectiveness of these from enhanced metabolism
CNS depressants: Additive CNS depression cyclophosphamide: Possibly reduced half-life and increased leukopenic activity of cyclophosphamide disopyramide: Possibly ineffectiveness of disopyramide doxycycline, fenoprofen: Shortened half-life of these griseofulvin: Possibly decreased absorption and effectiveness of griseofulvin guanadrel, guanethidine: Possibly increased orthostatic hypotension
haloperidol: Decreased seizure threshold, decreased blood haloperidol level ketamine (high doses): Increased risk of hypotension and respiratory depression leucovorin: Interference with phenobarbital’s anticonvulsant effect levothyroxine, oral contraceptives, phenylbutazone, tricyclic antidepressants: Decreased effectiveness of these loxapine, phenothiazines,
thioxanthenes: Decreased seizure threshold
MAO inhibitors: Prolonged phenobarbital effects, possibly altered pattern of seizure activity maprotiline: Increased CNS depression, decreased seizure threshold at high doses, decreased phenobarbital effectiveness
methoxyflurane: Possibly hepatotoxicity and nephrotoxicity
methylphenidate: Increased risk of phenobarbital toxicity
mexiletine: Decreased blood mexiletine level oral anticoagulants: Decreased anticoagulant activity, increased risk of bleeding when phenobarbital is discontinued pituitary hormones (posterior): Increased risk of arrhythmias and coronary insufficiency primidone: Altered pattern of seizures, increased CNS effects of both valproate,
valproic acid: Decreased phenobarbital metabolism, increased risk of barbiturate toxicity
vitamin D: Decreased phenobarbital effectiveness xanthines: Increased xanthine metabolism, antagonized hypnotic effect of phenobarbital
alcohol use: Additive CNS depression

Side Efect

CNS: Anxiety, depression, dizziness, drowsiness, headache, irritability, lethargy, mood changes, paradoxical stimulation, sedation, vertigo
CV: Hypotension, sinus bradycardia
EENT: Miosis, ptosis
GI: Constipation, diarrhea, nausea, vomiting
GU: Decreased libido, impotence, sexual dysfunction
MS: Arthralgia, bone tenderness
RESP: Bronchospasm, respiratory depression
SKIN: Dermatitis, photosensitivity, rash, urticaria
Other: Injection site phlebitis (I.V.), physical and psychological dependence

Cautions

Be aware that phenobarbital shouldn’t be given during third trimester of pregnancy because repeated use can cause dependence in neonate. It also shouldn’t be given to breast-feeding women because it may cause CNS depression in infants.

Use I.V. route cautiously in patients with CV disease, hypotension, pulmonary disease, or shock because drug may cause adverse hemodynamic or respiratory effects.

Because drug can cause respiratory depression, assess respiratory rate and depth before use, especially in patient with bronchopneumonia, pulmonary disease, respiratory tract infection, or status asthmaticus.

Give elixir undiluted or mix with water, milk, or fruit juice. Use a calibrated device to measure doses.

If necessary, crush tablets and mix with food or fluids.

Reconstitute sterile powder with at least 10 ml sterile water for injection. Don’t use reconstituted solution if it fails to clear within 5 minutes. Further dilute prescribed dose with normal saline solution or D5W and infuse over 30 to 60 minutes.

Don’t give more rapidly than 60 mg/min by I.V. injection.

During I.V. use, monitor blood pressure, respiratory rate, and heart rate and rhythm. Anticipate increased risk of hypotension, even at recommended rate. Keep resuscitation equipment readily available.

During I.M. use, don’t inject more than 5 ml into any one I.M. site to prevent sterile abscess formation.

Be aware that drug may cause physical and psychological dependence.

Expect that phenobarbital’s CNS effects may exacerbate major depression, suicidal tendencies, or other mental disorders.

Take safety precautions for elderly patients, as appropriate, because they’re more likely to experience confusion, depression, and excitement as adverse CNS reactions.

Anticipate that phenobarbital may cause paradoxical stimulation in children.

Be aware that drug may trigger signs and symptoms in patients with acute intermittent porphyria. phenobarbital 818

PATIENT SAFTY

Instruct patient to take phenobarbital elixir undiluted or to mix it with water, milk, or fruit juice. Advise her to use a calibrated device to measure doses.

If patient has trouble swallowing tablets, suggest crushing and adding to food or fluid.

Caution patient about possible drowsiness and reduced alertness. Advise her to avoid potentially hazardous activities until drug’s CNS effects are known.

Urge patient to avoid alcohol during therapy.

Inform parents that a child may react with paradoxical excitement. Tell them to notify prescriber if this occurs.

Instruct woman to report suspected, known, or intended pregnancy. Advise against breast-feeding during therapy.

Category

Chemical class: Imidazoline
Therapeutic class: Antihypertensive, diagnostic aid, vasodilator

Pregnancy category: Not rated

Indications

To diagnose pheochromocytoma I.V. INJECTION
Adults. 2.5 mg as a single dose. After negative result, repeat test with 5-mg dose, as prescribed. Children. 1 mg as a single dose. After negative result, repeat test with 0.1-mg/kg dose, as prescribed. To manage hypertension before or during pheochromocytomectomy I.V. OR

IM

Adults. 5 mg 1 to 2 hr before surgery, repeated as needed and as prescribed. During surgery, 5 mg I.V., as ordered. Children. 1 mg 1 to 2 hr before surgery, repeated as needed and as prescribed. During surgery, 1 mg I.V., as ordered. To prevent dermal necrosis or sloughing after extravasation of I.V. norepinephrine I.V. INJECTION Adults,children,and infants. 10 mg/L of I.V. fluid that contains norepinephrine at rate determined by patient response. To treat dermal necrosis or sloughing after extravasation of I.V. norepinephrine INTRADERMAL INJECTION
Adults. 5 to 10 mg in 10 ml of normal saline solution infiltrated in affected area within 12 hr of extravasation. Children. 0.1 to 0.2 mg/kg. Maximum: 10 mg.

Mechanism of Action

Blocks the actions of circulating epinephrine and norepinephrine by antagonizing alpha1and alpha2receptors. Phentolamine causes peripheral vasodilation through direct relaxation of vascular smooth muscle and alpha blockade. Positive inotropic and chronotropic effects increase cardiac output. A positive inotropic effect primarily raises blood pressure, but in larger doses, phentolamine causes peripheral vasodilation and can reduce blood pressure. In patients with pheochromocytoma, phentolamine causes systolic and diastolic blood pressures to fall dramatically. In those without pheochromocytoma, it causes blood pressure to fall or rise slightly or remain the same.

Contraindications

Angina, hypersensitivity to phentolamine or its components, MI

Interactions

antihypertensives: Additive hypotensive effect dopamine: Antagonized vasopressor activity of dopamine epinephrine, methoxamine, norepinephrine, phenylephrine: Inhibited alpha adrenergic effects of these metaraminol: Possibly decreased vasopressor effect of metaraminol
alcohol use: Additive vasodilation, increased risk of hypotension and tachycardia

Side Efect

CNS: Dizziness
CV: Angina; arrhythmias, including tachycardia; hypotension
EENT: Nasal congestion
GI: Diarrhea, nausea, vomiting
GU: Ejaculation disorders, priapism
MS: Muscle weakness
SKIN: Flushing

Cautions

Reconstitute each 5-mg vial phentolamine with 1 ml sterile water for injection.

Use reconstituted solution immediately; don’t store unused portion.

Dilute 5 to 10 mg of reconstituted solution in 500 ml D5W. Inspect drug for particles and discoloration before administering.

When diagnosing pheochromocytoma, hold nonessential , as ordered, for at least 24 hours (preferably 48 to 72) before test.

Before giving I.V. test dose for pheochromocytoma, place patient in supine position and assess baseline blood pressure with readings every 10 minutes for at least 30 minutes.

In pheochromocytoma, expect excessive hypotension after patient receives drug.

Take safety precautions according to facility policy if patient experiences dizziness.

PATIENT SAFTY

Instruct patient to move slowly after phentolamine administration to minimize dizziness and avoid falls.

Category

Chemical class: Sympathomimetic amine
Therapeutic class: Antiarrhythmic, decongestant, vasoconstrictor, vasopressor

Pregnancy category: C

(parenteral), Not rated (nasal)

Indications

To manage mild to moderate hypotension I.V. INJECTION
Adults. Initial: 0.1 to 0.5 mg. Usual: 0.2 mg, repeated no more than every 10 to 15 min. I.M.OR SUBCUTANEOUS INJECTION
Adults. Initial: 1 to 5 mg. Usual: 2 to 5 mg (range, 1 to 10 mg), repeated no more than every 10 to 15 min, as prescribed. To treat severe hypotension or shock

IV

Adults. Initial: 100 to 180 mcg/min (0.1 to 0.18 mg/min) until blood pressure is stable. Maintenance: 40 to 60 mcg/min (0.04 to 0.06 mg/min). Infusion concentration and flow rate adjusted as prescribed, based on patient response. To prevent hypotension during spinal anesthesia I.M.OR SUBCUTANEOUS INJECTION
Adults. 2 to 3 mg 3 or 4 min before injection of spinal anesthetic. Children. 0.5 to 1 mg for each 11.3 kg (25 lb). To treat hypotension during spinal anesthesia I.V. INJECTION
Adults. Initial: 0.2 mg, increased by no more than 0.2 mg, as prescribed. Maximum: 0.5 mg/dose. Children. 0.5 to 1 mg for each 11.3 kg (25 lb). To treat paroxysmal supraventricular tachycardia I.V. INJECTION
Adults. Initial: Up to 0.5 mg by rapid injection; later doses increased 0.1 to 0.2 mg higher than preceding dose, as prescribed. Maximum: 1 mg/dose. To treat sinus, nasal, and eustachian tube congestion NASAL JELLY OR SOLUTION Adults and children age 12 and over.2 or 3 drops or sprays of 0.25% or 0.5% solution every 4 hr, p.r.n., or small quantity of 0.5% nasal jelly in each nostril every 3 to 4 hr, p.r.n. A 1% solution may be used for severe congestion. Children ages 6 to 12. 2 or 3 drops or sprays of 0.25% solution in each nostril every 4 hr, p.r.n. Children ages 2 to 6. 2 or 3 drops or sprays of 0.125% or 0.16% solution in each nostril every 4 hr, p.r.n.

Mechanism of Action

Directly stimulates alpha-adrenergic receptors and inhibits the intracellular enzyme adenyl cyclase, which then inhibits production of cAMP. Inhibition of cAMP causes arterial and venous constriction and increases peripheral vascular resistance and systolic blood pressure. With greater-thantherapeutic doses, phenylephrine directly stimulates beta-adrenergic receptors in the myocardium, which increases activity of adenyl cyclase and produces positive inotropic and chronotropic effect. Intranasal use directly stimulates alpha-adrenergic receptors on the nasal mucosa, constricting local vessels and decreasing blood flow and mucosal edema. Route Onset Peak Duration I.V. Immediate Unknown 15–20 min I.M. 10–15 min Unknown 30 min– 2 hr SubQ 10–15 min Unknown 50 min– 1 hr Nasal Unknown Unknown 30 min– 4 hr

Incompatibilities

Don’t combine nasal form with alkalies, butacaine, ferrous salts, metals, or oxidizing agents.

Contraindications

Hypersensitivity to bisulfites, phenylephrine, or their components; severe coronary artery disease or hypertension; use within 14 days of MAO inhibitor; ventricular tachycardia

Interactions

alpha blockers, haloperidol, loxapine, phenothiazines,
thioxanthenes: Possibly decreased vasoconstrictor effect of phenylephrine; decreased decongestant effect of nasal phenylephrine (with phenothiazines) antihypertensives, diuretics: Possibly decreased antihypertensive effects atropine: Possibly enhanced vasopressor effect of phenylephrine
beta blockers: Decreased therapeutic effects of both bretylium: Possibly potentiated vasopressor effect and arrhythmias doxapram: Increased vasopressor effect of both ergot alkaloids: Possibly cerebral blood vessel rupture, increased vasopressor effect, peripheral vascular ischemia, and gangrene (with ergotamine) guanadrel, guanethidine: Increased vasopressor effect of phenylephrine, increased risk of severe hypertension and arrhythmias hydrocarbon inhalation anesthetics: Increased risk of serious arrhythmias
MAO inhibitors: Increased and prolonged cardiac stimulation, increased vasopressor effect, increased risk of severe cardiovascular and cerebrovascular effects, hyperpyrexia, vomiting maprotiline, tricyclic antidepressants: Increased risk of severe cardiovascular effects (including arrhythmias, hyperpyrexia, severe hypertension); possibly increased or decreased sensitivity to I.V. phenylephrine mecamylamine, methyldopa: Decreased hypotensive effects of these , increased vasopressor effect of phenylephrine nitrates: Possibly decreased vasopressor effect of phenylephrine and decreased antianginal effect of nitrates oxytocin: Possibly severe, persistent hypertension phenoxybenzamine: Decreased vasoconstrictor effect of phenylephrine, possibly hypotension and tachycardia
theophylline: Possibly enhanced toxicity (including cardiotoxicity); decreased theophylline level (with nasal phenylephrine) thyroid hormones: Increased cardiovascular effects of both urinary acidifiers: Possibly increased elimination and decreased therapeutic effects (with nasal phenylephrine) urinary alkalizers: Possibly decreased elimination and toxic effects (with nasal phenylephrine)

Side Efect

CNS: Dizziness, headache, insomnia, nervousness, paresthesia, restlessness, sleep disturbance (nasal), tremor, weakness
CV: Angina, bradycardia, hypertension, hypotension, palpitations, peripheral vasoconstriction that may lead to necrosis or gangrene, tachycardia, ventricular arrhythmias
EENT: Burning, dry, or stinging nasal mucosa; rebound congestion; and rhinitis (nasal forms)
GI: Nausea, vomiting
RESP: Dyspnea
SKIN: Extravasation with tissue necrosis and sloughing, pallor
Other: Allergic reaction

Cautions

Don’t dilute phenylephrine for I.M. or subcutaneous use.

To reduce the risk of tissue extravasation, don’t inject subcutaneous drug intradermally.

For I.V. use, dilute with D5W or sodium chloride for injection and prepare as prescribed—usually 10 mg/500 ml.

After nasal application, rinse spray bottle tip or nasal dropper with hot water and dry with clean tissue. Wipe tip of nasal jelly tube with clean tissue.

To prevent transmission of infection, don’t use nasal form on more than one patient.

Assess for signs and symptoms of angina, arrhythmias, and hypertension because phenylephrine may increase myocardial oxygen demand and the risk of proarrhythmias and blood pressure changes.
WARNING If patient has thyroid disease, watch for increased sensitivity to catecholamines and possible thyrotoxicity or cardiotoxicity.
WARNING Be aware that extravasation may cause tissue necrosis, gangrene, and other reactions around injection site. Expect to use phentolamine if extravasation occurs.

PATIENT SAFTY

If patient uses nasal form, explain that excessive use may cause rebound congestion. Urge her not to exceed recommended dosage and to use for only 3 to 5 days.

Teach patient who uses nasal form how to care for spray bottle, dropper, or tube.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Category

Chemical class: Hydantoin derivative
Therapeutic class: Anticonvulsant

Pregnancy category: C

Indications

To treat tonic-clonic, simple, or complex partial seizures in patients who have had no prior treatment CHEWABLE , ORAL SUSPENSION (PHENYTOIN) Adults and adolescents. Initial: 125 mg suspension or 100 to 125 mg tablet t.i.d., adjusted every 7 to 10 days as needed and tolerated. Children. Initial: 5 mg/kg daily in divided doses b.i.d. or t.i.d., adjusted as needed and tolerated. Maintenance: 4 to 8 mg/kg daily in divided doses b.i.d. or t.i.d. Maximum: 300 mg daily. EXTENDED (PHENYTOIN SODIUM) Adults and adolescents. Initial: 100 mg t.i.d., adjusted every 7 to 10 days as needed and tolerated. Maintenance: Once seizures are controlled, adjusted dosage given daily if needed and tolerated.
DOSAGE ADJUSTMENT For hospitalized patients without hepatic or renal disease, oral loading dose of 400 mg followed in 2 hr by 300 mg and then in 2 more hr by another 300 mg for a total of 1 g. Children. Initial: 5 mg/kg daily in divided doses b.i.d. or t.i.d., adjusted as needed and tolerated. Maintenance: 4 to 8 mg/kg daily in divided doses b.i.d. or t.i.d. Maximum: 300 mg daily. PROMPT (PHENYTOIN SODIUM) Adults and adolescents. 100 mg t.i.d., adjusted every 7 to 10 days as needed and tolerated. Children. Initial: 5 mg/kg daily in divided doses b.i.d. or t.i.d., adjusted as needed and tolerated. Maintenance: 4 to 8 mg/kg daily in divided doses b.i.d. or t.i.d. Maximum: 300 mg daily. To treat status epilepticus I.V. INJECTION (PHENYTOIN SODIUM) Adults and adolescents. Initial: 15 to 20 mg/kg by slow push in 50 ml sodium chloride injection at no more than 50 mg/ min. Maintenance: Beginning within 12 to 24 hr of initial dose, 5 mg/kg daily P.O. in divided doses b.i.d. to q.i.d., or 100 mg I.V. every 6 to 8 hr. phenytoin 822 Children. 15 to 20 mg/kg at no more than 1 mg/kg/min. Maximum: 50 mg/min.
DOSAGE ADJUSTMENT For elderly or very ill patients and those with CV or hepatic disease, dosage reduced to 25 mg/min, as prescribed, or possibly as low as 5 to 10 mg/ min to reduce the risk of

Side Efect

. To prevent or treat seizures during neurosurgery I.V. INJECTION (PHENYTOIN SODIUM)
Adults. 100 to 200 mg every 4 hr at no more than 50 mg/min during or immediately after neurosurgery.

Mechanism of Action

Limits the spread of seizure activity and the start of new seizures by regulating voltagedependent sodium and calcium channels in neurons, inhibiting calcium movement across neuronal membranes, and enhancing sodium-potassium ATP activity in neurons and glial cells. These actions all help stabilize the neurons.

Incompatibilities

Don’t mix phenytoin in same syringe with any other or with any I.V. solutions other than sodium chloride for injection because precipitate will form.

Contraindications

Adams-Stokes syndrome, hypersensitivity to phenytoin or its components, SA block, secondor third-degree heart block, sinus bradycardia

Interactions

acetaminophen: Possibly hepatotoxicity, decreased acetaminophen effects activated charcoal, antacids, calcium salts, enteral feedings, sucralfate: Decreased absorption of oral phenytoin allopurinol, benzodiazepines, chloramphenicol, cimetidine, disulfiram, fluconazole, isoniazid, itraconazole, methylphenidate, metronidazole, miconazole, omeprazole, phenacemide, ranitidine, sulfonamides, trazodone, trimethoprim: Decreased metabolism and increased effects of phenytoin amiodarone, ticlopidine: Possibly increased blood phenytoin level antifungals (azole): Increased blood phenytoin level, decreased blood antifungal level antineoplastics, nitrofurantoin, pyridoxine: Decreased phenytoin effects barbiturates: Variable effects on blood phenytoin level bupropion, clozapine, loxapine, MAO inhibitors, maprotiline, molindone, phenothiazines, pimozide, thioxanthenes, tricyclic antidepressants: Decreased seizure threshold, decreased anticonvulsant effects calcium channel blockers: Increased metabolism and decreased effects of these , possibly increased blood phenytoin level carbamazepine: Decreased blood level and effects of carbamazepine, possibly phenytoin toxicity carbonic anhydrase inhibitors: Increased risk of osteopenia from phenytoin chlordiazepoxide, diazepam: Possibly increased blood phenytoin level, decreased effects of these clonazepam: Possibly decreased blood level and effects of clonazepam, possibly phenytoin toxicity corticosteroids, cyclosporine, dicumarol, digoxin, disopyramide, doxycycline, estrogens, furosemide, lamotrigine, levodopa, methadone, metyrapone, mexiletine, oral contraceptives, quinidine, sirolimus, tacrolimus,
theophylline: Increased metabolism and decreased effects of these dopamine: Increased risk of severe hypotension and bradycardia (with I.V. phenytoin) fluoxetine: Increased blood phenytoin level and risk of phenytoin toxicity folic acid, leucovorin: Decreased blood phenytoin level, increased risk of seizures
haloperidol: Decreased effects of haloperidol, decreased anticonvulsant effect of phenytoin halothane anesthetics: Increased risk of hepatotoxicity and phenytoin toxicity ifosfamide: Decreased phenytoin effects, possibly increased toxicity influenza virus vaccine: Possibly decreased phenytoin effects insulin, oral antidiabetic : Possibly hyperglycemia, increased blood phenytoin level (with tolbutamide) levonorgestrel, mebendazole, streptozocin, sulfonylureas: Decreased effects of these lidocaine, propranolol (possibly other beta blockers): Increased cardiac depressant effects (with I.V. phenytoin), possibly decreased blood level and increased adverse effects of phenytoin lithium: Increased risk of lithium toxicity, increased risk of neurologic symptoms with normal blood lithium level meperidine: Increased metabolism and decreased effects of meperidine, possibly meperidine toxicity methadone: Possibly increased metabolism of methadone and withdrawal symptoms neuromuscular blockers: Shorter duration of action and decreased effects of neuromuscular blockers oral anticoagulants: Decreased metabolism and increased effects of phenytoin; early increase and then decrease in anticoagulation paroxetine: Decreased bioavailability of both phenylbutazone, salicylates: Increased phenytoin effects, possibly phenytoin toxicity primidone: Increased primidone effects, possibly primidone toxicity
rifampin: Increased hepatic metabolism of phenytoin
valproic acid: Possibly decreased phenytoin metabolism, resulting in increased phenytoin effects; possibly decreased blood valproic acid level
vitamin D: Possibly decreased vitamin D effects, resulting in rickets or osteomalacia (with long-term use of phenytoin)
alcohol use: Additive CNS depression, increased phenytoin clearance

Side Efect

CNS: Ataxia, confusion, depression, dizziness, drowsiness, excitement, fever, headache, involuntary motor activity, lethargy, nervousness, peripheral neuropathy, restlessness, slurred speech, suicidal ideation, tremor, weakness
CV: Cardiac arrest, hypotension, vasculitis
EENT: Amblyopia, conjunctivitis, diplopia, earache, epistaxis, eye pain, gingival hyperplasia, hearing loss, loss of taste, nystagmus, pharyngitis, photophobia, rhinitis, sinusitis, taste perversion, tinnitus
ENDO: Gynecomastia, hyperglycemia
GI: Abdominal pain, anorexia, constipation, diarrhea, epigastric pain, hepatic dysfunction, hepatic necrosis, hepatitis, nausea, vomiting
GU: Glycosuria, priapism, renal failure
HEME: Acute intermittent porphyria (exacerbation), agranulocytosis, anemia, eosinophilia, leukopenia, pancytopenia, thrombocytopenia
MS: Arthralgia, arthropathy, bone fractures, muscle twitching, osteomalacia, polymyositis
RESP: Apnea, asthma, bronchitis, cough, dyspnea, hypoxia, increased sputum production, pneumonia, pneumothorax, pulmonary fibrosis
SKIN: Exfoliative dermatitis, jaundice, maculopapular or morbilliform rash, purpuric dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, unusual hair growth, urticaria
Other: Facial feature enlargement, injection site pain, lupus-like symptoms, lymphadenopathy, polyarteritis, weight gain or loss

Cautions

WARNING Patients of Asian ancestry who have the genetic allelic variant HLA-B 1502 develop serious and sometimes fatal dermatologic reactions ten times more often than people without this variant when given carbamazepine, another antiepileptic drug. Because early data suggest a similar effect with phenytoin, this drug shouldn’t be used as a substitute for carbamazepine in these patients.

Be aware that preferred administration routes for phenytoin are oral and I.V. injection. With I.M. administration, phenytoin has a variable absorption rate.

If patient has difficulty swallowing, open prompt (rapid-release) capsules and mix contents with food or fluid.

Shake oral suspension before measuring dose, and use a calibrated measuring device.

To minimize GI distress, give phenytoin with or just after meals.

Inspect I.V. form for particles and discoloration before administering.
WARNING Avoid rapid I.V. injection because it may cause cardiac arrest, CNS depression, or severe hypotension.

To decrease vein irritation, follow I.V. injection with flush of sodium chloride for injection through same I.V. catheter.

Continuously monitor ECG tracings and blood pressure when administering I.V. phenytoin.

Frequently assess I.V. site for signs of extravasation because drug can cause tissue necrosis. phenytoin 824

If patient has an NG tube in place, minimize drug absorption by polyvinyl chloride tubing by diluting suspension threefold with sodium chloride for injection, D5W, or sterile water. After administration, flush tube with at least 20 ml diluent.

Separate oral phenytoin administration by at least 2 hours from antacids and calcium salts.

Expect continuous enteral feedings to disrupt phenytoin absorption and, possibly, reduce blood phenytoin level. Discontinue tube feedings 1 to 2 hours before and after phenytoin administration, as prescribed. Anticipate giving increased phenytoin doses to compensate for reduced bioavailability during continuous tube feedings.

Monitor phenytoin level. Therapeutic level ranges from 10 to 20 mcg/L.
WARNING Monitor patient’s hematologic status during therapy because phenytoin can cause blood dyscrasias. A patient with a history of agranulocytosis, leukopenia, or pancytopenia may have an increased risk of infection because phenytoin can cause myelosuppression.

Anticipate that drug may worsen intermittent porphyria.

Frequently monitor blood glucose level of patient with diabetes mellitus because drug can stimulate glucagon secretion and impair insulin secretion, either of which can raise blood glucose level.

Monitor thyroid hormone levels in patient receiving thyroid replacement therapy because phenytoin may decrease circulating thyroid hormone levels and increase thyroid-stimulating hormone level.

Be aware that long-term phenytoin therapy may increase patient’s requirements for folic acid or vitamin D supplements. However, keep in mind that a diet high in folic acid may decrease seizure control.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

Category

Chemical class: Salicylic acid derivative
Therapeutic class: Anticholinergic antidote, cholinesterase inhibitor

Pregnancy category: Not rated

Indications

To counteract toxic anticholinergic effects (anticholinergic syndrome) I.V. OR

IM

Adults and adolescents. 0.5 to 2 mg at no more than 1 mg/min; then 1 to 4 mg, repeated every 20 to 30 min as needed and as prescribed. Children. 0.02 mg/kg I.V., at no more than 0.5 mg/min, repeated every 5 to 10 min as prescribed. Maximum: 2 mg/dose.

Mechanism of Action

Inhibits destruction of acetylcholine by acetylcholinesterase. This action increases acetylcholine concentration at cholinergic transmission sites and prolongs and exaggerates effects of acetylcholine that are blocked by toxic doses of anticholinergics. Route Onset Peak Duration I.V. 3–8 min 5 min 30–60 min I.M. 3–8 min 20–30 min 30–60 min

Contraindications

Asthma; cardiovascular disease; diabetes mellitus; gangrene; GI or GU obstruction; hypersensitivity to physostigmine, sulfites, or their components

Interactions

choline esters: Enhanced effects of carbachol and bethanechol with concurrent use of physostigmine, enhanced effects of acetylcholine and methacholine with prior use of physostigmine succinylcholine: Prolonged neuromuscular paralysis

Side Efect

CNS: CNS stimulation, fatigue, hallucinations, restlessness, seizures (with too-rapid I.V. delivery), weakness
CV: Bradycardia (with too-rapid I.V. delivery), irregular heartbeat, palpitations
EENT: Increased salivation, lacrimation, miosis
GI: Abdominal pain, diarrhea, nausea, vomiting
GU: Urinary urgency
MS: Muscle twitching
RESP: Bronchospasm, chest tightness, dyspnea (with too-rapid I.V. administration), increased bronchial secretions, wheezing
SKIN: Diaphoresis

Cautions

Use physostigmine cautiously in patients with bradycardia, epilepsy, or Parkinson’s disease.

Avoid rapid I.V. delivery, which may lead to bradycardia, respiratory distress, or seizures.

Check pulse and respiratory rates, blood pressure, and neurologic status often.

Monitor ECG tracing during I.V. use.

Closely monitor patient with asthma for asthma attack because physostigmine may precipitate attack by causing bronchoconstriction.

Watch for seizures in patient with a history of seizures because physostigmine can induce seizures by stimulating CNS.
WARNING Be alert for life-threatening cholinergic crisis, which may indicate physostigmine overdose and may include confusion, diaphoresis, hypotension, miosis, muscle weakness, nausea, paralysis (including respiratory paralysis), salivation, seizures, sinus bradycardia, and vomiting. If you detect such signs, prepare to give atropine (the antidote) and use resuscitation equipment. Keep in mind that atropine counteracts only muscarinic cholinergic effects; paralytic effects may continue.

PATIENT SAFTY

Reassure patient that vital signs will be monitored often to help prevent or detect

Side Efect

.

Instruct patient to notify prescriber at once about evidence of cholinergic crisis.

Category

Chemical class: Nonselective beta blocker
Therapeutic class: Antihypertensive

Pregnancy category: B

Indications

To manage hypertension
Adults. Initial: 5 mg b.i.d., increased by 10 mg daily every 3 to 4 wk, as prescribed. Maintenance: 10 to 30 mg daily. Maximum: 60 mg daily (U.S.), 45 mg daily (Canada). Route Onset Peak Duration P.O. Unknown 1–2 hr Up to 24 hr

Mechanism of Action

Blocks sympathetic stimulation of beta1 receptors in the heart and beta2receptors in vascular and bronchial smooth muscle by competing with adrenergic neurotransmitpindolol 826 ters, such as catecholamines. Pindolol’s negative chronotropic effects slow the resting heart rate and reduce exercise-induced tachycardia. Its negative inotropic effects reduce cardiac output, myocardial contractility, systolic and diastolic blood pressure, and myocardial oxygen consumption during stress or exercise. Among beta blockers, pindolol has the most intrinsic sympathomimetic activity and nonselective antagonism.

Contraindications

Advanced AV block; asthma; bronchospasm; cardiogenic shock; heart failure; hepatic disease; hypersensitivity to pindolol, other beta blockers, or their components; hypotension (with systolic pressure less than 100 mm Hg); sinus bradycardia

Interactions

allergy extracts or immunotherapy, iodinated contrast media: Increased risk of systemic reaction or anaphylaxis aluminum salts, barbiturates, calcium salts, certain penicillins, cholestyramine, colestipol, NSAIDs, rifampin, salicylates, sulfinpyrazone: Decreased blood level and effects of pindolol antihypertensives: Additive hypotensive effect beta blockers, digoxin: Increased risk of bradycardia calcium channel blockers,
quinidine: Possibly increased effects of both , symptomatic bradycardia (with diltiazem or verapamil), excessive hypertension or heart failure (with nifedipine)
cimetidine: Increased blood pindolol level epinephrine: Possibly hypertension followed by bradycardia ergotamine: Possibly severe peripheral vasoconstriction with pain and cyanosis estrogens: Decreased antihypertensive effect fentanyl, fentanyl derivatives: Risk of bradycardia after anesthesia induction insulin, oral antidiabetic : Masked symptoms of hypoglycemia, increased risk of hyperglycemia lidocaine: Increased risk of lidocaine toxicity
MAO inhibitors: Possibly hypertension neuromuscular blockers: Possibly increased or prolonged neuromuscular blockade phenothiazines: Increased blood levels of both
phenytoin: Possibly increased cardiac depressant effects prazosin, reserpine: Increased risk of orthostatic hypotension, bradycardia (with reserpine) quinolones: Possibly increased bioavailability of pindolol xanthines: Possibly decreased effects of both , decreased xanthine clearance

Side Efect

CNS: Anxiety, confusion, depression, dizziness, fatigue, fever, hallucinations, hypothermia, insomnia, memory loss, paresthesia, peripheral neuropathy, stroke, syncope, weakness
CV: Arrhythmias (including AV block and bradycardia), chest pain, decreased peripheral circulation, heart failure, hyperlipidemia, hypotension, MI, orthostatic hypotension, peripheral edema and ischemia, thrombosis of renal or mesenteric artery
EENT: Pharyngitis
ENDO: Hyperglycemia, hypoglycemia
GI: Colitis (ischemic), constipation, diarrhea, elevated liver function test results, gastritis, nausea, pancreatitis, vomiting
GU: Cystitis, decreased libido, renal colic, renal failure, urinary frequency, urine retention, UTI
HEME: Agranulocytosis, bleeding, eosinophilia, leukopenia, nonthrombocytopenic purpura, thrombocytopenia, thrombocytopenic purpura, unusual bleeding or bruising
MS: Arthralgia, back pain
RESP: Bronchospasm, pulmonary edema, pulmonary emboli
SKIN: Acne; alopecia; crusted, red, or scaly skin; diaphoresis; eczema; exfoliative dermatitis; hyperpigmentation; pruritus; purpura; rash
Other: Angioedema, positive ANA titer

Cautions

Check blood pressure and pulse rate often, especially at start of pindolol therapy. Also monitor fluid intake and output and daily weight, and assess for evidence of heart failure, such as dyspnea, edema, fatigue, and jugular vein distention.

Be aware that drug shouldn’t be stopped abruptly because MI, myocardial ischemia, severe hypertension, or ventricular arrhythmias may result.

Expect to discontinue drug up to 2 days before surgery, as prescribed, to reduce the risk of heart failure.

Assess distal circulation and peripheral pulses in patient with Raynaud’s phenomenon or other peripheral vascular disorder because drug can worsen these conditions.

Be aware that pindolol can mask tachycardia from hyperthyroidism; abrupt withdrawal can cause thyroid storm. Drug also may potentiate diplopia and muscle weakness in patient with myasthenia gravis; decrease blood glucose level, prolong or mask symptoms of hypoglycemia, and promote hyperglycemia in patient with diabetes mellitus; and worsen psoriasis.

PATIENT SAFTY

Instruct patient to weigh herself daily during pindolol therapy and to notify prescriber if she gains more than 2 lb (0.9 kg) in 1 day or 5 lb (2.3 kg) in 1 week.

Caution patient not to stop drug abruptly.

Advise patient to rise slowly from a seated or lying position to minimize effects of orthostatic hypotension.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to contact prescriber about bleeding or bruising, cough at night, depression, dizziness, edema, rash, shortness of breath, slow pulse rate, or sore throat.

Advise diabetic patient to monitor her blood glucose level more often during pindolol therapy because drug may mask symptoms of hypoglycemia.

Inform patient with psoriasis that drug may aggravate this condition.

Category

Chemical class: Thiazolidinedione
Therapeutic class: Antidiabetic

Pregnancy category: C

Indications

To achieve glucose control in type 2 diabetes mellitus as monotherapy or in combination with insulin, metformin, or a sulfonylurea
Adults. Initial: 15 or 30 mg daily. Maximum: 45 mg daily.
DOSAGE ADJUSTMENT For patients taking insulin, insulin dosage decreased by 10% to 25%, as prescribed, once glucose level reaches 100 mg/dl or less. If hypoglycemia occurs, dosage of any concurrent antidiabetic is reduced, as prescribed.

Mechanism of Action

Decreases insulin resistance by enhancing the sensitivity of insulin-dependent tissues, such as adipose tissue, skeletal muscle, and the liver, and reduces glucose output from the liver. Drug activates peroxisome proliferator-activated receptor-gamma (PPARg) receptors, which modulate transcription of insulin-responsive genes involved in glucose control and lipid metabolism. In this way, pioglitazone reduces hyperglycemia, hyperinsulinemia, and hypertriglyceridemia in patients with type 2 diabetes mellitus and insulin resistance. However, to work effectively, pioglitazone needs endogenous insulin. Unlike sulfonylureas, it doesn’t increase pancreatic insulin secretion.

Contraindications

Diabetic ketoacidosis, hypersensitivity to pioglitazone or its components heart falure, severe hepatic dysfunction, type 1 diabetes mellitus

Interactions

gemfibrozil,
rifampin: Possibly altered glucose control
ketoconazole: Possibly decreased metabolism of pioglitazone oral contraceptives: Possibly decreased effectiveness of oral contraceptives

Side Efect

CNS: Headache
CV: Congestive heart failure, edema
EENT: Blurred vision, decreased visual acuity, macular edema, pharyngitis, sinusitis, tooth disorders
HEME: Decreased hemoglobin level and hematocrit
MS: Fractures, myalgia
RESP: Upper respiratory tract infection
Other: Weight gain

Cautions

Be aware that pioglitazone isn’t recommended for patients with symptopmatic heart failure.

Be prepared to monitor liver function test results before therapy begins, every 2 months during first year, and annually thereafter, as ordered, because drug is extensively metabolized in the liver. Expect to stop drug if jaundice develops or ALT values exceed 2.5 times normal.
WARNING Monitor patient for signs and symptoms of congestive heart failure— such as shortness of breath, rapid weight gain, or edema—because pioglitazone can cause fluid retention that may lead to or worsen heart failure. Notify prescriber immediately of any deterioration in the patient’s cardiac status, and expect to discontinue the drug, as ordered.

Assess for signs and symptoms of hypoglycemia, especially if patient is also taking another antidiabetic drug.

Monitor fasting glucose level, as ordered, to evaluate effectiveness of therapy.

Monitor glycosylated hemoglobin level to assess drug’s long-term effectiveness.

PATIENT SAFTY

Stress the need for patient to continue exercise program, diet control, and weight management during pioglitazone therapy.

Advise patient to notify prescriber immediately if she experiences shortness of breath, fluid retention, or sudden weight gain because drug may need to be discontinued.

Urge patient to report vision changes promptly and expect to have an eye examination by an ophthalmologist regardless of when the last examination occurred.

Instruct patient to keep appointments for liver function tests, as ordered, typically every 2 months during first year of therapy and annually thereafter.

Inform female patient who uses oral contraceptives that drug decreases their effectiveness; suggest that she use another method of contraception while taking pioglitazone.

Also inform female patient that she may be at risk for fractures during pioglitazone therapy, and urge her to take safety precautions to prevent falls and other injuries.

Category

Chemical class: Piperazine derivative of ampicillin, acylureidopenicillin
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat moderate to severe bacterial infections, including bone and joint infections, gynecologic infections, intraabdominal infections, lower respiratory tract infections, septicemia, and skin and soft-tissue infections, caused by susceptible strains of Acinetobacter species, anaerobic cocci, Bacteroides species, Enterobacter species, Escherichia coli, Haemophilus influenzae, Klebsiella species, Proteus species, Pseudomonas aeruginosa, and Serratia species

IV

Adults and adolescents. 12 to 18 g daily or 200 to 300 mg/kg daily in divided doses every 4 to 6 hr. Maximum: 24 g daily. To treat bacterial meningitis

IV

Adults and adolescents. 4 g every 4 hr or 75 mg/kg every 6 hr. Maximum: 24 g daily. To treat uncomplicated UTI and community-acquired pneumonia caused by susceptible organisms, including E. coli, Klebsiella species, and Serratia species

IV

,

IM

Adults. 6 to 8 g daily or 100 to 125 mg/kg daily in divided doses every 6 to 12 hr. To treat complicated UTI caused by susceptible organisms, including Acinetobacter species, Klebsiella species, and Serratia species

IV

Adults. 8 to 16 g daily or 125 to 200 mg/kg daily in divided doses every 6 to 8 hr. To treat uncomplicated gonorrhea caused by susceptible strains of Neisseria gonorrhoeae
I.M.INJECTION
Adults. 2 g as a single dose 30 min after 1-g dose of probenecid P.O. To provide surgical prophylaxis in intraabdominal procedures, including GI and biliary surgery

IV

Adults. 2 g 20 to 30 min before anesthesia, 2 g during surgery, and 2 g every 6 hr for 24 hr after surgery. To provide surgical prophylaxis in abdominal hysterectomy

IV

Adults. 2 g 20 to 30 min before anesthesia, 2 g just after surgery, and 2 g 6 hr later. To provide surgical prophylaxis in vaginal hysterectomy

IV

Adults. 2 g 20 to 30 min before anesthesia, then 2 g 6 and 12 hr after initial dose. To provide surgical prophylaxis in cesarean section

IV

Adults. 2 g after cord is clamped, then 2 g 4 and 8 hr after initial dose.

Mechanism of Action

Binds to specific penicillin-binding proteins and inhibits the third and final stage of bacterial cell wall synthesis by interfering with an autolysin inhibitor. Uninhibited autolytic enzymes destroy the cell wall and result in cell lysis.

Incompatibilities

Don’t mix piperacillin sodium in same container with aminoglycosides because of chemical incompatibility (depending on concentrations, diluents, pH, and temperature). Don’t mix with solutions that contain only sodium bicarbonate because of chemical instability.

Contraindications

Hypersensitivity to cephalosporins, penicillins, or their components

Interactions

aminoglycosides: Additive or synergistic effects against some bacteria, possibly mutual inactivation anti-inflammatory (including aspirin and NSAIDs), heparin, oral anticoagulants, platelet aggregation inhibitors, sulfinpyrazone, thrombolytics: Increased risk of bleeding hepatotoxic (including labetalol and rifampin): Increased risk of hepatotoxicity methotrexate: Increased blood methotrexate level and risk of toxicity probenecid: Increased blood piperacillin level and risk of toxicity vecuronium: Possibly prolonged perioperative neuromuscular blockade of vecuronium

Side Efect

CNS: Dizziness, fever, hallucinations, headache, lethargy, seizures, stroke
CV: Cardiac arrest, hypotension, palpitations, tachycardia, vasodilation, vasovagal reactions
EENT: Oral candidiasis, pharyngitis
GI: Diarrhea, epigastric distress, intestinal necrosis, nausea, pseudomembranous colitis, vomiting
GU: Hematuria, impotence, nephritis, neurogenic bladder, priapism, proteinuria, renal failure, vaginal candidiasis
HEME: Agranulocytosis, eosinophilia, hemolytic anemia, leukopenia, neutropenia, pancytopenia, prolonged bleeding time, thrombocytopenia
MS: Arthralgia
RESP: Dyspnea, pulmonary embolism, pulmonary hypertension
SKIN: Exfoliative dermatitis, mottling, rash, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis; facial edema; hypokalemia; hyponatremia; injection site pain, phlebitis, and skin ulcer; superinfection

Cautions

Expect to obtain blood, sputum, or other samples for culture and sensitivity testing before giving piperacillin and to start therapy before results are available.

Be aware that sunlight may darken piperacillin powder for dilution but won’t alter drug potency.

For initial dilution for I.V. infusion, reconstitute each gram of drug with at least 5 ml sterile water for injection, sodium chloride for injection, D5W, dextrose 5% in normal saline solution, or bacteriostatic water that contains parabens or benzyl alcohol. Shake solution vigorously after adding diluent, and inspect for particles and discoloration before giving.

For further dilution, use sodium chloride for injection, D5W, dextrose 5% in normal saline solution, lactated Ringer’s solution, or dextran 6% in normal saline solution. Solutions diluted with lactated Ringer’s solution should be given within 2 hours.

For intermittent infusion, infuse appropriate dose over 20 to 30 minutes.

Give aminoglycosides 1 hour before or piperacillin sodium 830 after piperacillin; use a separate site, I.V. bag, and tubing.

For I.M. injection, reconstitute each gram of piperacillin with at least 2 ml of an appropriate diluent listed above.

Don’t give more than 2 g I.M. in one site. Use deltoid area cautiously and only if well developed to avoid injuring radial nerve.

Watch for bleeding or excessive bruising because drug can decrease platelet aggregation, especially in patients with renal failure. If bleeding occurs, notify prescriber and expect to stop piperacillin.

Monitor CBC regularly, as ordered, to detect hematologic abnormalities, such as leukopenia and neutropenia.

Monitor serum potassium level to detect hypokalemia from urinary potassium loss.

Check for diarrhea during and after therapy because it may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold piperacillin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Watch for hypersensitivity reactions, especially if patient has cystic fibrosis. Notify prescriber, and expect to stop drug.

PATIENT SAFTY

Advise patient to consult prescriber before using OTC during piperacillin therapy because of the risk of interactions.

Inform patient that increased bruising may occur if she takes anti-inflammatory during piperacillin therapy.

Advise patient to notify prescriber about signs of superinfection, such as white patches on tongue or in mouth.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and can be serious, requiring prompt treatment.

Instruct patient to complete full course of therapy, even if symptoms subside.

Category

Chemical class: Sympathomimetic amine
Therapeutic class: Bronchodilator

Pregnancy category: C

Indications

To prevent or treat bronchospasm caused by COPD, to treat bronchospasm caused by asthma ORAL INHALATION Adults and adolescents. 1 or 2 inhalations (200 to 400 mcg) every 4 to 6 hr. Maximum: 12 inhalations (2.4 mg) daily. Route Onset Peak Duration Oral inIn 5 min In 30–90 3–6 hr halation min

Mechanism of Action

Attaches to beta2receptors on bronchial cell membranes, which stimulates the intracellular enzyme adenyl cyclase to convert adenosine triphosphate (ATP) to cAMP. The increased intracellular level of cAMP relaxes bronchial smooth-muscle cells and inhibits histamine release. Pirbuterol also stabilizes mast cells and inhibits the release of histamine.

Contraindications

Hypersensitivity to pirbuterol or its components, tachycardia

Interactions

beta-adrenergic bronchodilators: Additive effects beta blockers (ophthalmic): Possibly decreased pirbuterol effects, increased risk of bronchospasm beta blockers (systemic): Decreased effects of both , increased risk of bronchospasm MAO inhibitors, tricyclic antidepressants: Potentiated cardiovascular effects

Side Efect

CNS: Anxiety, confusion, depression, dizziness, headache, nervousness, tiredness, tremor
CV: Arrhythmias (including PVCs and tachycardia), chest pain, ECG changes (including flattening of T waves, prolonged QT interval, and ST-segment depression), hypotension, palpitations
EENT: Dry mouth
GI: Abdominal cramps, diarrhea, nausea, vomiting
RESP: Bronchospasm, cough
SKIN: Alopecia, rash, urticaria
Other: Facial edema, hypokalemia

Cautions

For patient with a cardiovascular disorder, such as arrhythmia, hypertension, or ischemic cardiac disease, monitor blood pressure and heart rate and rhythm to detect significant changes after pirbuterol use.

Be aware that elderly patients have greater risk of

Side Efect

than younger
Adults.
WARNING Stop giving drug and notify prescriber immediately if patient has paradoxical bronchospasm, a life-threatening adverse reaction.

PATIENT SAFTY

Teach patient how to use an inhaler and spacer correctly, and urge her to keep the inhaler readily available at all times.

Recommend the use of an autohaler if patient has trouble coordinating inhalations with a regular inhaler.

Advise patient to clean the inhaler’s mouthpiece at least once daily.

Caution patient against overusing drug because doing so may increase adverse reactions.

Teach patient how to use peak flow meter and determine her personal best reading.
WARNING Advise patient to notify prescriber if symptoms worsen, if bronchospasm occurs more frequently, if she needs to use the inhaler more often, or if the inhaler becomes less effective.

Category

Chemical class: Oxicam derivative
Therapeutic class: Anti-inflammatory, antirheumatic

Pregnancy category: Not rated

Indications

To treat acute and chronic osteoarthritis and rheumatoid arthritis
Adults. Initial: 20 mg once daily or 10 mg b.i.d.

Mechanism of Action

Blocks the activity of cyclooxygenase, the enzyme needed for prostaglandin synthesis. Prostaglandins, important mediators of the inflammatory response, cause local vasodilation with swelling and pain. By blocking cyclooxygenase activity and inhibiting prostaglandins, this NSAID reduces inflammatory symptoms and pain. Route Onset Peak Duration P.O. Unknown Several Unknown days to 1 wk*

Contraindications

Angioedema, asthma, bronchospasm, nasal polyps, rhinitis, or urticaria induced by aspirin, iodides, or other NSAIDs; hypersensitivity to piroxicam or its components

Interactions

acetaminophen: Possibly increased adverse renal effects with long-term use of both antihypertensives: Possibly decreased or reversed effects of antihypertensives aspirin, other
NSAIDs: Increased risk of bleeding and adverse GI effects, possibly increased blood piroxicam level cefamandole, cefoperazone, cefotetan: Increased risk of hypoprothrombinemia and bleeding colchicine: Increased risk of GI bleeding, hemorrhage, and ulcers corticosteroids, potassium supplements: Increased risk of adverse GI effects cyclosporine: Increased risk of nephrotoxicity from both , increased blood cyclosporine level diuretics: Decreased antihypertensive, diuretic, and natriuretic effects of diuretics gold compounds, nephrotoxic : Increased risk of adverse renal effects heparin, oral anticoagulants, thrombolytics: Increased anticoagulant effects, increased risk of hemorrhage insulin, oral antidiabetic : Possibly increased hypoglycemic effect of these lithium: Possibly increased blood lithium * With severe inflammation, 2 wk or more. level and toxicity methotrexate: Decreased methotrexate clearance and increased risk of methotrexate toxicity platelet aggregation inhibitors: Increased risk of bleeding and GI ulceration or hemorrhage plicamycin,
valproic acid: Increased risk of hypoprothrombinemia and GI bleeding, hemorrhage, and ulceration probenecid: Possibly increased blood level, effectiveness, and risk of toxicity of piroxicam
alcohol use: Increased risk of adverse GI effects

Side Efect

CNS: Anxiety, aseptic meningitis, asthenia, cerebral hemorrhage, confusion, depression, dizziness, dream disturbances, drowsiness, fever, headache, insomnia, ischemic stroke, malaise, nervousness, paresthesia, somnolence, syncope, transient ischemic attack, tremor, vertigo
CV: Deep vein thrombosis, edema, heart failure, hypertension, MI, peripheral edema, tachycardia
EENT: Blurred vision, dry mouth, epistaxis, glossitis, stomatitis, tinnitus
ENDO: Hypoglycemia
GI: Abdominal pain; anorexia; constipation; diarrhea; elevated liver function test results; esophagitis; flatulence; gastritis; GI bleeding, perforation, or ulceration; heartburn; hematemesis; hepatitis; indigestion; jaundice; liver failure; melena; nausea; vomiting
GU: Acute renal failure, cystitis, dysuria, elevated serum creatinine level, hematuria, interstitial nephritis, nephrotic syndrome, oliguria, polyuria, proteinuria, renal failure or insufficiency
HEME: Agranulocytosis, anemia, aplastic anemia, coagulation abnormalities, eosinophilia, leukopenia, pancytopenia, thrombocytopenia
RESP: Asthma, dyspnea
SKIN: Alopecia, diaphoresis, ecchymosis, erythema, erythema multiforme, exfoliative dermatitis, photosensitivity, pruritus, purpura, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, flulike symptoms, hyperkalemia, infection, sepsis, weight loss or gain

Cautions

Administer piroxicam with food to decrease GI upset.

Use piroxicam with extreme caution in patients with a history of ulcer disease or GI bleeding because NSAIDs such as piroxicam increase risk of GI bleeding and ulceration. Expect to use piroxicam for the shortest time possible in these patients.

Be aware that serious GI tract ulceration, bleeding, and perforation may occur without
WARNING symptoms. Elderly patients are at greater risk. To minimize risk, give drug with food. If GI distress occurs, withhold drug and notify prescriber at once.

Use piroxicam cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.
WARNING Monitor patient closely for thrombotic events, including MI and stroke, because NSAIDs increase the risk.
WARNING If patient has bone marrow suppression or is receiving antineoplastic drug therapy, monitor laboratory results (including WBC count), and watch for evidence of infection because anti-inflammatory and antipyretic actions of piroxicam may mask signs and symptoms, such as fever and pain.

Especially if patient is elderly or taking drug long-term, watch for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results because, rarely, elevated levels may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in patients with heart failure, impaired renal function, or hepatic dysfunction; those taking diuretics or ACE inhibitors; and elderly patients because drug may cause renal failure.

Monitor CBC for decreased hemoglobin level and hematocrit because drug may worsen anemia.

Assess patient’s skin routinely for rash or other signs of hypersensitivity reaction because piroxicam and other NSAIDs may cause serious skin reactions without warning, even in patients with no history of NSAID hypersensitivity. Stop drug at first sign of reaction, and notify prescriber.
WARNING Be aware that drug may cause premature closure of ductus arteriosus in growing fetus during third trimester of pregnancy. Be prepared to suggest referral for high-risk pregnancy.

PATIENT SAFTY

Advise patient to take piroxicam with meals to minimize GI distress. Also direct her to take drug with a full glass of water and to remain upright for 30 minutes afterward to decrease risk of drug lodging in esophagus and causing irritation.

Instruct patient to swallow capsules whole and not to crush, break, chew, or open them.

Advise patient to avoid alcohol, aspirin, and other NSAIDs, unless prescribed, while taking piroxicam.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

If patient also takes an anticoagulant, advise her to watch for and immediately report bleeding problems, such as bloody or tarry stools and bloody vomitus.

If patient also takes insulin or an oral antidiabetic, advise her to closely monitor blood glucose level to prevent hypoglycemia. Urge her to carry candy or other simple sugars to treat mild hypoglycemia. Advise her to notify prescriber if hypoglycemic episodes are frequent or severe.

Explain that piroxicam may increase risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.

Tell patient that piroxicam may increase risk of serious adverse GI reactions; stress the need to seek immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.

Alert patient to possibility of rare but serious skin reactions. Urge her to seek immediate medical care for rash, blisters, itching, fever, or other signs of hypersensitivity.

Instruct female patient to consult prescriber if she becomes pregnant because drug may cause premature closure of ductus arteriosus in growing fetus.

Category

Chemical class: HMG-CoA reductase inhibitor
Therapeutic class: Antihyperlipidemic, statin

Pregnancy category: X

Indications

To decrease elevated total cholesterol, LDL, apolipoprotein B, and triglyceride levels and increase HDL level as adjunct to diet in patients with primary hyperlipidemia or mixed dyslipidemia
Adults. Initial: 2 mg once daily, increased as needed. Maximum: 4 mg once daily
DOSAGE ADJUSTMENT For patients with moderate renal impairment (glomerular filtration rate 30 to 60 ml/min/1.73m2) or patients receiving dialysis, initial dosage reduced to 1 mg once daily, with maximum of 2 mg once daily. For patients taking erythromycin, dosage shouldn’t exceed 1 mg daily; for patients taking rifampin, dosage shouldn’t exceed 2 mg daily. Route Onset Peak Duration P.O. Unknown 1 hr Unknown

Mechanism of Action

Reduces plasma cholesterol and lipoprotein levels by inhibiting HMG-CoA reductase and cholesterol synthesis in the liver. Consequently, number of LDL receptors on liver cells increases, and LDL uptake and breakdown are enhanced. With sustained inhibition of cholesterol synthesis in the liver, levels of very low-density lipoproteins are decreased.

Contraindications

Active liver disease (including unexplained persistent LFT elevation), breast-feeding, concurrent cyclosporine therapy, hypersensitivity to pitavastatin or its components, women who are pregnant or may become pregnant

Interactions

cyclosporine, erythromycin, lopinavir and ritonavir,
rifampin: Increased pitavastatin exposure fibrates such as gemfibrozil: Increased risk of myopathy niacin: Increased risk of adverse skeletal muscle effects

Side Efect

CNS: Headache
EENT: Nasopharyngitis
ENDO: Elevated blood glucose level
GI: Constipation, diarrhea, elevated liver enzyme levels
GU: Acute renal failure, myoglobinuria
MS: Arthralgia, back or extremity pain, myopathy, myositis, rhabdomyolysis
SKIN: Pruritus, rash, urticaria
Other: Elevated creatine phosphkinase level, influenza

Cautions

Be aware that pitavastatin isn’t recommended for patients with severe renal impairment who aren’t on dialysis and for patients currently receiving lopinavir and ritonavir therapy because of increased risk of serious adverse effects.

Note that pravastatin, another HMG-CoA reductase inhibitor, sounds similar to pitavastatin and could be confusing. Make sure of correct drug before giving.

Use pitavastatin cautiously in patients with risk factors for myopathy, such as age over 65, presence of renal impairment, being inadequately treated for hypothyroidism, or concurrent use of niacincontaining products or fibrates. Monitor patient throughout therapy for muscular complaints and an elevated blood creatine kinase level, as ordered. Drug should be discontinued if patient’s creatine kinase level becomes markedly elevated or myopathy is suspected or confirmed.

Expect liver function tests to be done before pitavastatin starts, after 6 and 12 weeks of therapy, with each dosage increase, and every 6 months thereafter.

Expect to monitor patient’s lipid levels after 4 weeks of therapy to determine drug effectiveness and periodically thereafter, as ordered. Expect dosage to be adjusted if lipid levels remain elevated.

PATIENT SAFTY

Stress that pitavastatin is an adjunct to, not a substitute for, a low-cholesterol diet.

Tell patient to take drug at the same time each day to maintain its effects.

Instruct patient to report unexplained muscle pain, tenderness, or weakness, especially if accompanied by malaise or fever.

Advise patient to limit alcohol ingestion while taking pitavastatin because alcoholinduced liver dysfunction may be difficult to differentiate from pitavastatin-induced liver dysfunction.

Instruct patient to consult prescriber before taking OTC niacin products because of increased risk of adverse muscle effects.

Caution women of childbearing age that drug is contraindicated in pregnancy because drug could be harmful to the baby. If pregnancy is suspected, patient should notify prescriber immediately.

Category

Chemical class: Bacillus polymyxa derivative
Therapeutic class: Antibiotic

Pregnancy category: Not rated

Indications

To treat infections resistant to less toxic , such as bacteremia, septicemia, and UTI caused by susceptible organisms, including Enterobacter aerogenes, Escherichia coli, Haemophilus influenzae, and Klebsiella pneumoniae

IV

Adults and children age 2 and over. 15,000 to 25,000 units/kg daily in divided doses every 12 hr or as a continuous infusion. Maximum: 2 million units daily. Infants and children under age 2. Up to 40,000 units/kg daily in divided doses every 12 hr or as a continuous infusion.
I.M.INJECTION Adults and children age 2 and over. 25,000 to 30,000 units/kg daily in divided doses every 4 to 6 hr. Maximum: 2 million units daily. Infants and children under age 2. Up to 40,000 units/kg daily in divided doses every 4 to 6 hr.
DOSAGE ADJUSTMENT Dosage reduced by 50% for patients with creatinine clearance of 5 to 20 ml/min/1.73 m2; by 85% for patients with creatinine clearance of less than 5 ml/min/ 1.73 m2. To prevent bacteriuria and bacteremia in patients with an indwelling catheter BLADDER IRRIGATION Adults and children age 2 and over. Combination of 200,000 units (20 mg) polymyxin B sulfate and 57 mg neomycin sulfate added to 1,000 ml normal saline solution daily as a continuous bladder irrigation for up to 10 days; rate adjusted as prescribed, based on patient’s urine output. To treat meningitis caused by susceptible strains of Pseudomonas aeruginosa or H. influenzae

INTRATHECAL

INJECTION Adults and children age 2 and over. 50,000 units daily for 3 to 4 days, then 50,000 units every other day for at least 2 wk after CSF cultures are negative and glucose content is normal. Infants and children under age 2. 20,000 units daily for 3 to 4 days, then 25,000 units every other day for at least 2 wk after CSF cultures are negative and glucose content is normal.

Mechanism of Action

Binds to cell membrane phospholipids in gram-negative bacteria, increasing permeability of cell membrane. Polymyxin B also acts as a cationic detergent, altering osmotic barrier of membrane and causing essential intracellular metabolites to leak out. Both actions lead to cell death.

Incompatibilities

Don’t mix polymyxin B sulfate with amphotericin B, calcium salts, chloramphenicol, chlorothiazide, heparin sodium, magnesium salts, nitrofurantoin, penicillins, prednisolone, and tetracyclines. They’re incompatible.

Contraindications

Hypersensitivity to polymyxin B or its components

Interactions

general anesthetics, neuromuscular blockers, skeletal muscle relaxants: Increased or prolonged skeletal muscle relaxation, possibly respiratory paralysis nephrotoxic and neurotoxic (such as aminoglycosides, amphotericin B, colistin, sodium citrate, streptomycin, tobramycin, and vancomycin): Increased risk of nephrotoxicity and neurotoxicity

Side Efect

CNS: Ataxia, confusion, dizziness, drowsiness, fever, giddiness, headache, increased leukocyte and protein levels in CSF, neurotoxicity, paresthesia (circumoral or peripheral), slurred speech
CV: Thrombophlebitis
EENT: Blurred vision, nystagmus
GU: Albuminuria, azotemia, cylindruria, decreased urine output, hematuria, nephrotoxicity
HEME: Eosinophilia
RESP: Respiratory muscle paralysis
SKIN: Rash, urticaria
Other: Anaphylaxis, drug-induced fever, facial flushing, injection site pain, stiff neck (with intrathecal injection), superinfection

Cautions

Be aware that patients receiving polymyxin B sulfate are hospitalized to allow appropriate supervision.

Obtain blood, urine, or other samples for culture and sensitivity tests, as ordered, before giving drug. Expect to start drug before results are known. Keep in mind that baseline renal function tests should have been performed before administration. Check test results, if available, and notify prescriber of abnormalities.

For I.M. injection, reconstitute sterile powder with 2 ml of sterile water for injection or sodium chloride for injection.

Be aware that I.M. route isn’t usually recommended (especially for infants and children) because it can cause severe pain at injection site.

For I.V. infusion, dissolve polymyxin B in 300 to 500 ml of D5W and infuse over 60 to 90 minutes.

For intrathecal route, add 10 ml sodium chloride for injection to polymyxin B vial.

Inspect for particles and discoloration before giving drug.

During therapy, monitor renal function, including BUN and serum creatinine levpolymyxin B sulfate 836 els, especially in patients with a history of renal insufficiency.
WARNING Be aware that declining urine output and rising BUN level suggest nephrotoxicity, which also is characterized by albuminuria, azotemia, cylindruria, excessive excretion of electrolytes, hematuria, leukocyturia, and rising blood drug level. Notify prescriber immediately if you detect any of these signs.
WARNING Notify prescriber immediately if patient experiences blurred vision, circumoral or peripheral paresthesia, confusion, dizziness, drowsiness, facial flushing, giddiness, myasthenia, nystagmus, or slurred speech. These may be signs of neurotoxicity, a serious adverse reaction that may lead to respiratory arrest or paralysis if untreated.

Assess for signs of superinfection, such as mouth sores, severe diarrhea, and white patches on tongue or in mouth, especially in debilitated or elderly patients.

Monitor fluid intake and output and provide adequate fluids to reduce the risk of nephrotoxicity.

PATIENT SAFTY

Encourage patient to maintain adequate fluid intake during polymyxin B therapy.

Instruct patient to notify prescriber at once about diarrhea, mouth sores, or vaginitis, possible early signs of superinfection.

Category

Chemical class: Triazole
Therapeutic class: Antifungal

Pregnancy category: C

Indications

To prevent invasive aspergillus and candida infections in patients at high risk because of severe immunocompromise from such conditions as graftversus-host disease with hematopoietic stem-cell transplant or hematologic malignancies with prolonged neutropenia from chemotherapy ORAL SUSPENSION
Adults. 200 mg (5 ml) t.i.d. until recovery from neutropenia or immunosuppression. To treat oropharyngeal candidiasis ORAL SUSPENSION
Adults. Initial: 100 mg (2.5 ml) b.i.d. on first day, followed by 100 mg (2.5 ml) once daily for 13 days. To treat oropharyngeal candidiasis refractory to itraconazole and or fluconazole ORAL SUSPENSION
Adults. 400 mg (10 ml) b.i.d. until underlying condition improves. Route Onset Peak Duration P.O. Unknown 3–5 hr Unknown

Mechanism of Action

Blocks synthesis of ergosterol, an essential component of fungal cell membrane, by inhibiting 14 alpha-demethylase, an enzyme needed for conversion of lanosterol to ergosterol. Lack of ergosterol increases cellular permeability, and cell contents leak.

Contraindications

Concurrent therapy with sirolimus; hypersensitivity to posaconazole, its components, or other azole antifungals; use with ergot alkaloids or CYP3A4 substrates such as astemizole, cisapride, halofantrine, pimozide, quinidine, and terfenadine

Interactions

astemizole, cisapride, halofantrine, pimozide, quinidine, terfenadine: Increased risk of prolonged QT interval and torsades de pointes atazanavir, calcium channel blockers, cyclosporine, midazolam, phenytoin, rifabutin, ritonavir, sirolimus, tacrolimus: Increased plasma levels of these , with increased risk of

Side Efect

cimetidine, efavirenz, phenytoin,
rifabutin: Possibly decreased plasma level of posaconazole digoxin: Increased risk of digitalis toxicity ergot alkaloids: Increased plasma ergot alkaloid level and increased risk of ergotism esomeprazole, metoclopramide: Possible breakthrough fungal infections HMG-CoA reductase inhibitors: Increased plasma statin level and increased risk of rhabdomyolysis
vinca alkaloids: Increased plasma vinca alkaloid level and increased risk of neurotoxicity

Side Efect

CNS: Anxiety, asthenia, dizziness, fatigue, fever, headache, insomnia, rigors, tremor, weakness
CV: Edema, hypertension, hypotension, QT-interval prolongation, tachycardia
EENT: Blurred vision, epistaxis, herpes simplex, mucositis, pharyngitis, taste perversion
ENDO: Hyperglycemia, hypocalcemia
GI: Abdominal pain, anorexia, bilirubinemia, constipation, diarrhea, dyspepsia, elevated liver enzyme levels, hepatomegaly, jaundice, nausea, vomiting
GU: Acute renal failure, elevated blood creatinine level, vaginal hemorrhage
HEME: Anemia, neutropenia, thrombocytopenia
MS: Arthralgia, back or musculoskeletal pain
RESP: Coughing, dyspnea, pneumonia, upper respiratory tract infection
SKIN: Diaphoresis, petechiae, pruritus, rash
Other: Bacteremia, cytomegalovirus infection, dehydration, hypokalemia, hypomagnesemia, weight loss

Cautions

Use cautiously in patients who have had a hypersensitivity reaction to other azoles because of risk for cross-sensitivity.

Use cautiously in patients with renal or hepatic dysfunction.

Use cautiously in patients with potentially proarrhythmic conditions because posaconazole may prolong QT interval.

Obtain baseline assessment of liver function and check periodically during therapy. If elevations occur or patient has evidence of abnormal liver function, notify prescriber.

PATIENT SAFTY

Advise patient to use the measuring spoon supplied by manufacturer and to rinse it with water after each use.

Instruct patient to take posaconazole with or within 20 minutes after a full meal or liquid nutritional supplement to increase drug absorption. Tell patient that he also may take posaconazole with an acidic carbonated beverage such as gingerale.

Tell patient to report severe diarrhea or vomiting because these conditions may interfere with drug effectiveness.

Category

Chemical class: Electrolyte cation
Therapeutic class: Electrolyte replacement

Pregnancy category: C

Indications

To prevent or treat hypokalemia in patients who can’t ingest sufficient dietary potassium or who are losing potassium because of a condition (such as hepatic cirrhosis or prolonged vomiting) or drug (such as potassium-wasting diuretics or certain antibiotics) EFFERVESCENT (POTASSIUM BICARBONATE) Adults and adolescents. 25 to 50 mEq/g once or twice daily, as needed and tolerated. Maximum: 100 mEq daily. EFFERVESCENT (POTASSIUM BICARBONATE AND POTASSIUM CHLORIDE) Adults and adolescents. 20, 25, or 50 mEq once or twice daily, as needed and tolerated. Maximum: 100 mEq daily. EFFERVESCENT (POTASSIUM BICARBONATE AND POTASSIUM CITRATE) Adults and adolescents. 25 or 50 mEq once or twice daily, as needed and tolerated. Maximum: 100 mEq daily. ELIXIR(POTASSIUM GLUCONATE) Adults and adolescents. 20 mEq b.i.d. to q.i.d., as needed and tolerated. Maximum: 100 mEq daily. Children. 2 to 3 mEq/kg daily in divided doses. (POTASSIUM CHLORIDE) Adults and adolescents. 40 to 100 mEq daily in divided doses b.i.d. or t.i.d. for treatment; 16 to 24 mEq daily in divided doses b.i.d. or t.i.d. for prevention. Maximum: 100 mEq daily. (POTASSIUM CHLORIDE) Adults and adolescents. 6.7 to 20 mEq t.i.d. Maximum: 100 mEq daily. GRANULE PACKETS(POTASSIUM BICARBONATE AND POTASSIUM CHLORIDE) Adults and adolescents. 20 mEq once or twice daily, as needed and tolerated. Maximum: 100 mEq daily. GRANULES FOR ORAL SUSPENSION(POTASSIUM CHLORIDE) Adults and adolescents. 20 mEq 1 to 5 times/ day, as needed. Maximum: 100 mEq daily.

ORALL

(POTASSIUM CHLORIDE) Adults and adolescents. 20 mEq once daily potassium 839 P to q.i.d., as needed and tolerated. Maximum: 100 mEq daily. Children. 1 to 3 mEq/kg daily in divided doses.

ORALL

(POTASSIUM GLUCONATE AND POTASSIUM CHLORIDE,POTASSIUM GLUCONATE AND POTASSIUM CITRATE) Adults and adolescents. 20 mEq b.i.d. to q.i.d., as needed and tolerated. Maximum: 100 mEq daily. Children. 2 to 3 mEq/kg daily in divided doses. POWDER PACKET FOR (POTASSIUM CHLORIDE)
Adults. 15 to 25 mEq b.i.d. to q.i.d., as needed and tolerated. Maximum: 100 mEq daily. Children. 1 to 3 mEq/kg daily in divided doses, as needed and tolerated. POWDER PACKET FOR(POTASSIUM GLUCONATE AND POTASSIUM CHLORIDE) Adults and adolescents. 20 mEq b.i.d. to q.i.d., as needed and tolerated. Maximum: 100 mEq daily. Children. 2 to 3 mEq/kg daily in divided doses. ORAL TRIKATES SOLUTION(POTASSIUM ACETATE, POTASSIUM BICARBONATE, AND POTASSIUM CITRATE) Adults and adolescents. 15 mEq t.i.d. to q.i.d., as needed and tolerated. Maximum: 100 mEq daily. Children. 2 to 3 mEq/kg daily in divided doses. (POTASSIUM GLUCONATE) Adults and adolescents. 5 to 10 mEq b.i.d. to q.i.d., as needed and tolerated. Maximum: 100 mEq daily.

IV

(POTASSIUM ACETATE AND POTASSIUM CHLORIDE) Adults and adolescents with serum potassium level above 2.5 mEq/L. Up to 10 mEq/ hr. Maximum: 200 mEq daily. Adults and adolescents with serum potassium level below 2 mEq/L, ECG changes, or paralysis.Up to 20 mEq/hr. Maximum: 400 mEq daily. Children. 3 mEq/kg daily.
DOSAGE ADJUSTMENT Dosage adjusted as prescribed based on patient’s ECG patterns and serum potassium level. To treat renal tubular acidosis with calcium stones, hypocitraturic calcium oxalate nephrolithiasis of any etiology, and uric acid lithiasis with or without calcium stones (POTASSIUM CITRATE)
Adults. For patients with severe hypocitraturia, 15 mEq four times daily with meals or 20 mEq three times daily with meals. For patients with mild to moderate hypocitraturia, 10 mEq three times daily with meals.

Mechanism of Action

Acts as the major cation in intracellular fluid, activating many enzymatic reactions essential for physiologic processes, including nerve impulse transmission and cardiac and skeletal muscle contraction. Potassium also helps maintain electroneutrality in cells by controlling exchange of intracellular and extracellular ions. It also helps maintain normal renal function and acid-base balance.

Incompatibilities

Don’t mix potassium chloride for injection in same syringe with amino acid solutions, lipid solutions, or mannitol because these may precipitate from solution. Administration with blood or blood products can cause lysis of infused RBCs.

Contraindications

Acute dehydration, Addison’s disease (untreated), concurrent use of potassiumsparing diuretics, crush syndrome, disorders that may delay drug passing through GI tract (potassium citrate), heat cramps, hyperkalemia, hypersensitivity to potassium salts or their components, peptic ulcer disease (potassium citrate), renal impairment with azotemia or oliguria, severe hemolytic anemia, UTI (potassium citrate)

Interactions

ACE inhibitors, beta blockers, blood products, cyclosporine, heparin, NSAIDs, potassiumcontaining , potassium-sparing diuretics: Increased risk of hyperkalemia amphotericin B, corticosteroids (glucocorticoids, mineralocorticoids), gentamicin, penicillins, polymyxin B: Possibly hypokalemia anticholinergics, with anticholinergic activity: Increased risk of GI ulceration, stricture, and perforation calcium salts (parenteral): Possibly arrhythmias digoxin: Increased risk of digitalis toxicity potassium 840 insulin, laxatives, sodium bicarbonate: Decreased serum potassium level sodium polystyrene sulfonate: Possibly decreased serum potassium level and fluid retention thiazide diuretics: Possibly hyperkalemia when diuretic is discontinued low-salt milk, salt substitutes: Increased risk of hyperkalemia

Side Efect

CNS: Confusion, paralysis, paresthesia, weakness
CV: Arrhythmias, ECG changes
EENT: Throat pain when swallowing
GI: Abdominal pain; bloody stools; diarrhea; flatulence; GI bleeding, perforation, or ulceration; intestinal obstruction; nausea; vomiting
RESP: Dyspnea
SKIN: Rash
Other: Hyperkalemia

Cautions

Administer oral potassium with or immediately after meals.

Mix potassium chloride for oral solution or potassium gluconate elixir in cold water, orange juice, tomato juice (if patient isn’t sodium restricted), or apple juice, and stir for 1 full minute before administering.

Mix potassium bicarbonate, potassium bicarbonate and potassium chloride, and potassium bicarbonate and potassium citrate effervescent tablets with cold water and allow to dissolve completely.

Be aware that liquid form of oral potassium is prescribed for patients with delayed gastric emptying, esophageal compression, or intestinal obstruction or stricture to decrease the risk of tissue damage.
WARNING Be aware that direct injection of a potassium concentrate may be immediately fatal. Dilute potassium concentrate for injection with adequate volume of solution before I.V. use. Maximum suggested concentration is 40 mEq/L, although stronger concentrations (up to 80 mEq/L) may be used for severe hypokalemia. Inappropriate solutions or improper technique may cause extravasation, fever, hyperkalemia, hypervolemia, I.V. site infection, phlebitis, venospasm, and venous thrombosis.

Infuse potassium slowly to avoid phlebitis and decrease risk of adverse cardiac reactions. Keep in mind that different forms of potassium salts contain different amounts of elemental potassium per gram and that not all forms are dosage equivalent.

Monitor serum potassium level before and during administration of I.V. potassium.
WARNING Be aware that some forms of potassium contain tartrazine, which may cause an allergic reaction, such as asthma. Some forms may also contain aluminum, which may become toxic in a patient with impaired renal function.

Regularly assess patient for signs of hypokalemia, such as arrhythmias, fatigue, and weakness, and for signs of hyperkalemia, such as arrhythmias, confusion, dyspnea, and paresthesia.

Because adequate renal function is needed for potassium supplementation, monitor serum creatinine level and urine output during administration. Notify prescriber about signs of decreased renal function.

PATIENT SAFTY

Inform patient that potassium is part of a normal diet and that most meats, sea, fruits, and vegetables contain sufficient potassium to meet recommended daily intake. Also advise her not to exceed recommended daily amount of potassium.

Teach patient the correct way to take prescribed potassium. This can vary from swallowing a tablet with a full glass of water to mixing certain preparations with half to full glass of cold water or juice.

Caution patient not to crush or chew forms unless instructed otherwise.

Instruct patient to take drug with or right after food.

Teach patient how to take her radial pulse, and advise her to notify prescriber about significant changes in heart rate or rhythm.

Advise patient to watch stools for changes in color and consistency and to notify prescriber if they become black, tarry, or red.

Inform patient that although she may see waxy form of tablet in stools, she has received all of the potassium.

Urge patient to keep follow-up laboratory appointments as directed by prescriber to determine serum potassium level.

Category

Chemical class: Iodine
Therapeutic class: Antithyroid, radiation protectant

Pregnancy category: D

Indications

To prepare for thyroidectomy

ORALL

Adults and children. 50 to 250 mg t.i.d. for 10 to 14 days before surgery. To manage thyrotoxic crisis

ORALL

Adults. 50 to 250 mg t.i.d. or 500 mg every 4 hr. To protect thyroid gland during radiation exposure

ORALL

, SYRUP, Adults and adolescents. 100 to 150 mg 24 hr before administration of or exposure to radioactive isotopes of iodine and daily for 3 to 10 days afterward. Maximum: 12 g daily. Children age 1 and over. 130 mg daily for 10 days after administration of or exposure to radioactive isotopes of iodine. Children under age 1. 65 mg daily for 10 days after administration of or exposure to radioactive isotopes of iodine. Route Onset Peak Duration P.O.* 24 hr 10–15 days Up to 6 wk

Mechanism of Action

Inhibits release of thyroid hormone into circulation, thus alleviating symptoms caused by excessive thyroid hormone stimulation. Potassium iodide also blocks thyroid uptake of radioactive iodine isotopes released as a result of radiation exposure.

Contraindications

Acute bronchitis, Addison’s disease, dehydration, heat cramps, hyperkalemia, hypersensitivity to iodides or their components, hyperthyroidism, iodism, renal impairment, tuberculosis

Interactions

antithyroid , lithium: Increased risk of hypothyroidism and goiter captopril, enalapril, lisinopril, potassiumsparing diuretics: Increased risk of hyperkalemia

Side Efect

CNS: Confusion, fatigue, headache, heaviness or weakness in legs, paresthesia
CV: Irregular heartbeat
EENT: Burning in mouth or throat, increased salivation, metallic taste, sore teeth or gums
GI: Diarrhea, epigastric pain, indigestion, nausea, vomiting
HEME: Eosinophilia
MS: Arthralgia
SKIN: Acneiform lesions, urticaria
Other: Angioedema, lymphadenopathy

Cautions

Be aware that potassium iodide shouldn’t be given to patients with tuberculosis because drug may cause pulmonary irritation and increased secretions.
WARNING Monitor serum potassium level regularly in patients with renal impairment because of the risk of hyperkalemia.

Monitor thyroid function test results periodically to assess drug’s effectiveness.

PATIENT SAFTY

Advise patient taking potassium iodide oral solution or syrup to use a calibrated measuring device to ensure accurate doses.

Urge patient to mix solution or syrup in a full glass (8 oz) of water, fruit juice, milk, or broth to improve taste and lessen GI reactions. Advise patient taking tablet form to dissolve each tablet in half a glass (4 oz) of water or milk before ingestion.

If crystals form in solution, advise patient to place the closed container in warm water and gently shake to dissolve.

Instruct patient to discard bottle and obtain a new one if solution turns brownish yellow.

Category

Chemical class: Anion, soluble salts
Therapeutic class: Antiurolithic, electrolyte replenisher, urinary acidifier

Pregnancy category: C

Indications

As adjunct to treat UTI, to prevent renal calculus formation MONOBASIC (POTASSIUM PHOSPHATES) Adults and adolescents. 1 g in 180 to 240 ml water q.i.d., after meals and at bedtime. MONOBASIC (POTASSIUM AND SODIUM PHOSPHATES) Adults and adolescents. 250 mg in 240 ml water q.i.d., after meals and at bedtime. Dosage interval may be increased to every 2 hr if urine is difficult to acidify. Maximum: 2 g/24 hr. To prevent or treat hypophosphatemia (POTASSIUM PHOSPHATES) Adults and children age 4 and over. 1.45 g in 75 ml water or juice q.i.d., after meals and at bedtime. Children up to age 4. 200 mg in 60 ml water or juice q.i.d., after meals and at bedtime. (POTASSIUM AND SODIUM PHOSPHATES) Adults and children age 4 and over. 1.25 g in 75 ml water or juice q.i.d., after meals and at bedtime. Children up to age 4. 200 mg in 60 ml water or fruit juice q.i.d., after meals and at bedtime. MONOBASIC (POTASSIUM PHOSPHATES) Adults and children age 4 and over.1 g in 180 to 240 ml water q.i.d., after meals and at bedtime. Children up to age 4. 200 mg in 60 ml water q.i.d., after meals and at bedtime. MONOBASIC (POTASSIUM AND SODIUM PHOSPHATES) Adults and children age 4 and over. 250 mg in 240 ml water q.i.d., after meals and at bedtime. Children up to age 4. 200 mg in 60 ml water q.i.d., after meals and at bedtime.

ORALL

(POTASSIUM PHOSPHATES, POTASSIUM AND SODIUM PHOSPHATES) Adults and children age 4 and over. 250 mg q.i.d., after meals and at bedtime. Children up to age 4. 200 mg q.i.d., after meals and at bedtime. (POTASSIUM AND SODIUM PHOSPHATES) Adults and children age 4 and over. 250 mg in a full glass of water q.i.d., after meals and at bedtime. Children up to age 4. 200 mg in 60 ml water q.i.d., after meals and at bedtime.

IV

(SODIUM PHOSPHATES) Adults and adolescents. 10 to 15 mmol (310 to 465 mg) daily. Children. 1.5 to 2 mmol (46.5 to 62 mg)/kg daily.

Mechanism of Action

Reverses symptoms of hypophosphatemia by replenishing the body’s supply of phosphate; acidifies urine by causing hydrogen to be exchanged for sodium in renal distal tubule; and inhibits formation of calcium renal calculi by preventing solidification of calcium oxalate.

Incompatibilities

Don’t add phosphates to calciumor magnesium-containing solutions because precipitate may form.

Contraindications

Hyperkalemia (potassium formulations), hypernatremia (sodium formulations), hyperphosphatemia, magnesium ammonium phosphate urolithiasis accompanied by infection, severe renal insufficiency, UTI caused by urea-splitting organisms

Interactions

ACE inhibitors, cyclosporine, heparin (longterm use), NSAIDs, potassium-containing , potassium-sparing diuretics: Increased risk of hyperkalemia (potassium forms only) aluminumor magnesium-containing antacids: Possibly impaired phosphate absorption anabolic steroids, androgens, corticosteroids, estrogens: Increased risk of edema (sodium formulations only) calcium-containing : Increased risk of potassium phosphates 843 P calcium deposition in soft tissues iron supplements: Decreased absorption of oral iron phosphate-containing ,
vitamin D: Increased risk of hyperphosphatemia salicylates: Increased blood salicylate level zinc supplements: Reduced zinc absorption low-salt milk, salt substitutes: Increased risk of hyperkalemia oxalates (in spinach and rhubarb), phyates (in bran and whole grains): Decreased absorption of phosphate

Side Efect

CNS: Anxiety, confusion, dizziness, fatigue, headache, paresthesia, seizures, tremor, weakness
CV: Arrhythmias, edema of legs, tachycardia
GI: Diarrhea, epigastric pain, nausea, thirst, vomiting
GU: Decreased urine output
MS: Muscle cramps or weakness
RESP: Dyspnea
Other: Hyperkalemia, hypernatremia, hyperphosphatemia, hypocalcemia, weight gain

Cautions

Monitor serum phosphorus level, as appropriate, in patient who receives phosphates and has a condition that may be associated with elevated phosphorus level, such as chronic renal disease, hypoparathyroidism, and rhabdomyolysis; phosphates may further increase serum phosphorus level.

Monitor serum calcium level, as appropriate, in patient who receives phosphates and has a condition that may be associated with a low calcium level, such as acute pancreatitis, chronic renal disease, hypoparathyroidism, osteomalacia, rhabdomyolysis, and rickets; phosphates may further decrease serum calcium level.

Monitor serum potassium level, as appropriate, if patient who receives potassium phosphate has a condition linked to elevated potassium level, such as acute dehydration, adrenal insufficiency, extensive tissue breakdown (as in severe burns), myotonia congenita, pancreatitis, rhabdomyolysis, and severe renal insufficiency; she may have increased risk of hyperkalemia.

Monitor serum sodium level in patient who receives sodium phosphates and has a condition that may be worsened by sodium excess, such as heart failure, hypernatremia, hypertension, peripheral or pulmonary edema, preeclampsia, renal impairment, and severe hepatic disease.

Monitor urine pH, as ordered, to assess effectiveness of drug used to acidify urine.

When administering sodium phosphates, monitor ECG tracing frequently during I.V. infusion to detect arrhythmias.

PATIENT SAFTY

Instruct patient to take phosphates after meals to avoid GI upset and decrease laxative effect.

Stress importance of not swallowing capsules or tablets whole; instead, advise patient to soak tablets in water or fruit juice for 2 to 3 minutes to dissolve them.

Suggest chilling diluted drug to improve flavor, but caution against freezing.

Encourage increased intake of fluids (8 oz/ hour, if not contraindicated) to prevent renal calculi.

Urge patient to notify prescriber immediately about muscle weakness or cramps, unexplained weight gain,or shortness of breath.

Instruct patient who needs an iron supplement to take it 1 to 2 hours after taking phosphates.

Category

Chemical class: Quaternary ammonium oxime
Therapeutic class: Anticholinesterase antidote

Pregnancy category: C

Indications

As adjunct to reverse organophosphate pesticide toxicity

IV

, I.M. OR SUBCUTANEOUS INJECTION
Adults. Initial: 1 to 2 g in 100 ml normal saline solution infused over 15 to 30 min, pralidoxime chloride 844 given concurrently with atropine 2 to 6 mg every 5 to 60 min until muscarinic signs and symptoms disappear; may be repeated in 1 hr and then every 3 to 8 hr if muscle weakness persists. If I.V. route isn’t feasible, administer I.M. or subcutaneously. Children. Initial: 20 mg/kg in 100 ml normal saline solution infused over 15 to 30 min, given concurrently with atropine (dosage individualized); may be repeated in 1 hr and then every 3 to 8 hr if muscle weakness persists. If I.V. route isn’t feasible, administer I.M. or subcutaneously. To treat anticholinesterase overdose secondary to myasthenic (including ambenonium, neostigmine, and pyridostigmine) I.V. INJECTION
Adults. Initial: 1 to 2 g, followed by 250 mg every 5 min. To treat exposure to nerve agents I.V. INJECTION
Adults. Initial: 1 atropine-containing autoinjector followed by 1 pralidoximecontaining autoinjector as soon as atropine’s effects are evident; both injections repeated every 15 min for 2 additional doses if nerve agent symptoms persist.
DOSAGE ADJUSTMENT Dosage reduced for patients with renal insufficiency.

Mechanism of Action

Reverses muscle paralysis by removing phosphoryl group from inhibited cholinesterase molecules at neuromuscular junction of skeletal and respiratory muscles. Reactivation of cholinesterase restores body’s ability to metabolize acetylcholine, which is inhibited by organophosphate pesticides, anticholinesterase overdose, or nerve agent poisoning.

Contraindications

Hypersensitivity to pralidoxime chloride or its components

Interactions

aminophylline, morphine, phenothiazines, reserpine, succinylcholine,
theophylline: Increased symptoms of organophosphate poisoning barbiturates: Potentiated barbiturate effects

Side Efect

CNS: Dizziness, drowsiness, headache
CV: Increased systolic and diastolic blood pressure, tachycardia
EENT: Accommodation disturbances, blurred vision, diplopia
GI: Nausea, vomiting
MS: Muscle weakness
RESP: Hyperventilation
Other: Injection site pain

Cautions

Be aware that pralidoxime must be given within 36 hours of toxicity to be effective.

Use drug with extreme caution in patients with myasthenia gravis being treated for organophosphate poisoning because pralidoxime may precipitate myasthenic crisis.

Reconstitute drug according to manufacturer’s guidelines and administration route.

For intermittent infusion, further dilute with normal saline solution to 100 ml and infuse over 15 to 30 minutes.

Avoid too-rapid delivery, which may cause hypertension, laryngospasm, muscle spasms, neuromuscular blockade, and tachycardia. Also be sure to avoid intradermal injection.

Closely monitor neuromuscular status during therapy.

Monitor BUN and serum creatinine levels, as appropriate, in patients with renal insufficiency because drug is excreted in urine.

When pralidoxime is administered with atropine, expect signs of atropination, such as dry mouth and nose, flushing, mydriasis, and tachycardia, to occur earlier than might be expected when atropine is given alone.

PATIENT SAFTY

Inform patient receiving I.M. pralidoxime that she’ll experience pain at the injection site for 40 to 60 minutes afterward.

Reassure patient that she’ll be closely monitored throughout therapy.

Category

Chemical class: Benzothiazolamine derivative pramipexole dihydrochloride 845 P
Therapeutic class: Antidyskinetic

Pregnancy category: C

Indications

To treat Parkinson’s disease, with or without concurrent levodopa therapy
Adults. Initial: 0.125 mg t.i.d. for 1 wk, increased weekly thereafter as follows: for week 2, 0.25 mg t.i.d.; for week 3, 0.5 mg t.i.d.; for week 4, 0.75 mg t.i.d.; for week 5, 1 mg t.i.d.; for week 6, 1.25 mg t.i.d.; and for week 7, 1.5 mg t.i.d. Maintenance: 1.5 to 4.5 mg daily in divided doses t.i.d. Maximum: 4.5 mg daily.
DOSAGE ADJUSTMENT For patients with renal impairment, dosage reduced as follows: for creatinine clearance of 35 to 59 ml/min/1.73 m2, initial dose of 0.125 mg b.i.d., maximum of 3 mg daily; for creatinine clearance of 15 to 34 ml/min/1.73 m2, initial dose of 0.125 mg daily, maximum of 1.5 mg daily. Drug shouldn’t be given to patients with creatinine clearance of less than 15 ml/min/1.73 m2. To treat restless legs syndrome
Adults. Initial: 0.125 mg once daily, 2 to 3 hours before bedtime. Increased in 4 to 7 days to 0.25 mg once daily 2 to 3 hours before bedtime as needed. Further increased in 4 to 7 days to 0.5 mg once daily 2 to 3 hours before bedtime, as needed.
DOSAGE ADJUSTMENT For patients with moderate to severe renal impairment (creatinine clearance 20 to 60 ml/min/1.73 m2) dosage interval for titration, if needed, increased to 14 days.

Mechanism of Action

May stimulate dopamine receptors in the brain, thereby easing symptoms of Parkinson’s disease, which is thought to be caused by a dopamine deficiency.

Contraindications

Hypersensitivity to pramipexole or its components

Interactions

carbidopa, levodopa: Possibly increased peak blood levodopa level and potentiation of levodopa’s dopaminergic adverse effects diltiazem, quinidine, quinine, ranitidine, triamterene, verapamil: Decreased pramipexole clearance haloperidol, metoclopramide, phenothiazines,
thioxanthenes: Decreased pramipexole effectiveness

Side Efect

CNS: Abnormal behavior, amnesia, anxiety, asthenia, confusion, dream disturbances, drowsiness, dyskinesia, dystonia, fatigue, fever, hallucinations, headache, insomnia, malaise, paranoia, restlessness, syncope
CV: Edema, orthostatic hypotension
EENT: Diplopia, dry mouth, rhinitis, vision changes
GI: Anorexia,constipation,dysphagia,nausea
GU: Altered libido, impotence, urinary frequency, urinary incontinence
MS: Arthralgia, myalgia, myasthenia
RESP: Pneumonia
SKIN: Diaphoresis, rash
Other: Eating disorders (binge or compulsive eating, hyperphagia), intense urges for certain activities (such as gambling and sex), weight gain or loss

Cautions

Use pramipexole cautiously in patients with hallucinations, hypotension, or retinal problems (such as macular degeneration). Drug may worsen these conditions.

Also use cautiously in patients with renal impairment because pramipexole elimination may be decreased.

Take safety precautions per facility policy until drug’s CNS effects are known.

Avoid stopping pramipexole abruptly because doing so may cause a symptom complex resembling neuroleptic malignant syndrome and consisting of hyperpyrexia, muscle rigidity, altered level of consciousness, and autonomic instability.

Assess patient for skin changes regularly because melanomas may occur at a higher rate in patients with Parkinson’s disease. It isn’t clear if this is a result of the disease or used to treat it.

PATIENT SAFTY

Advise patient to take pramipexole with meals if nausea occurs.

Caution patient about possible dizziness, drowsiness, or light-headedness, which may result from orthostatic hypotension. Advise her not to rise quickly from a lying or sitting position to minimize these effects.

Instruct patient to notify prescriber immediately about vision problems or urinary frequency or incontinence.

Inform patient that improvement in motor performance and activities of daily living may take 2 to 3 weeks.

Urge patient to have regular skin examinations by a dermatologist or other qualified health professional.

Advise patient to notify prescriber about intense urges, as for gambling or sex. Dosage may need to be reduced or drug discontinued.

Category

Chemical class: Synthetic analogue of human amylin, a pancreatic beta cell hormone
Therapeutic class: Antidiabetic

Pregnancy category: C

Indications

To achieve euglycemia in patients with type 1 diabetes who use mealtime insulin therapy but have not achieved desired glucose control SUBCUTANEOUS INJECTION
Adults. Initial: 15 mcg just before major meals with 50% reduced dosage of preprandial rapid-acting or short-acting insulin, including fixed-mix insulins such as 70/30. When nausea has abated at least 3 days, dosage increased in increments of 15 mcg. Maintenance: 30 to 60 mcg before major meals.
DOSAGE ADJUSTMENT Dosage decreased to 30 mcg if nausea occurs and persists at higher dosages. To achieve euglycemia in patients with type 2 diabetes who use mealtime insulin, with or without a sulfonylurea and/or metformin, and have not achieved desire glucose control SUBCUTANEOUS INJECTION
Adults. Initial: 60 mcg immediately before major meals combined with dosage reduction of preprandial rapid-acting or shortacting insulin, including fixed-mix insulins such as 70/30, by 50%. When nausea has been absent for 3 to 7 days, dosage increased to 120 mcg before major meals.
DOSAGE ADJUSTMENT Dosage decreased to 60 mcg before major meals if nausea occurs and persists with 120-mcg dosage. Route Onset Peak Duration SubQ Unknown 19–21 min 3 hr

Mechanism of Action

Slows the rate at which food is released from stomach to small intestine, thus reducing initial postprandial rise in serum glucose level. Pramlintide also suppresses glucagon secretion and promotes satiety, thus furthering weight loss, which also lowers serum glucose level. Pramlintide is a synthetic analogue of amylin, a naturally occurring neuroendocrine hormone secreted with insulin by pancreatic beta cells. In diabetes, secretion of insulin and amylin is reduced or absent.

Contraindications

Gastroparesis, hypersensitivity to pramlintide, cresol or its components; hypoglycemia unawareness

Incompatibilities

Don’t mix in same syringe as insulin because pharmacokinetic parameters of pramlintide become altered.

Interactions

that alter GI motility (such as anticholinergics) or slow intestinal absorption of nutrients (such as alpha-glucosidase inhibitors): Altered effects of these oral : Delayed absorption

Side Efect

CNS: Dizziness, fatigue, headache
EENT: Blurred vision, pharyngitis
ENDO: Insulin-induced hypoglycemia
GI: Abdominal pain, anorexia, nausea, vomiting
MS: Arthralgia
RESP: Coughing
SKIN: Diaphoresis
Other: Hypersensitivity reactions; local injection site reaction, such as redness, swelling, or pruritus

Cautions

Because of the risks involved with pramlintide therapy, insulin-using patients with type 1 or 2 diabetes must have failed to achieve adequate glycemic control despite individualized insulin management and must be receiving ongoing care with guidance of insulin prescriber and a diabetes educator before pramlintide is prescribed.

Expect that certain patients won’t be prescribed pramlintide because its risks may outweigh its benefits. These include patients with poor compliance with current insulin regimen, poor compliance with monitoring blood glucose level, a glycosylated hemoglobin greater than 9%, recurrent severe hypoglycemia that required assistance during past 6 months, hypoglycemia unawareness, gastroparesis, concurrent therapy with that stimulate GI motility, and pediatric patients.

Before pramlintide therapy starts, make sure patient’s pre-meal insulin dosage has been reduced by 50%.

Give drug immediately before main meals.

Monitor patient’s preand post-meal blood glucose levels regularly to determine effectiveness of pramlintide and insulin therapy and to detect hypoglycemia.

For 3 hours after each dose of pramlintide, monitor patient closely for hypoglycemia, which may be severe, especially in patients with type 1 diabetes. Effects may include hunger, headache, sweating, tremor, irritability, and trouble concentrating. They may occur with a rapid decrease in blood glucose level regardless of glucose values.

Although pramlintide doesn’t cause hypoglycemia, it’s use with insulin increases the risk of insulin-induced severe hypoglycemia, which can result in loss of consciousness, coma, or seizures. If hypoglycemia occurs, provide supportive care, including glucagon if prescribed, and notify prescriber. Expect insulin dosage accompanying pramlintide to be reduced.

Keep in mind that early
WARNING symptoms of hypoglycemia may be different or less severe if patient has had diabetes for a long time; has diabetic nerve disease; takes a beta blocker, clonidine, guanethidine, or reserpine; or is under intensified diabetes control.

Closely monitor patients taking oral antidiabetics, ACE inhibitors, disopyramide, fibrates, fluoxetine, MAO inhibitors, pentoxifylline, propoxyphene, salicylates, or sulfonamide antibiotics because of an increased risk of hypoglycemia.

Expect pramlintide to be stopped if patient develops recurrent hypoglycemia that requires medical assistance, develops persistent nausea, or becomes noncompliant with therapy or follow-up visits.

PATIENT SAFTY

Alert patient that insulin-induced hypoglycemia may occur within 3 hours of injecting pramlintide. Review signs and symptoms and appropriate treatment. Tell patient to notify prescriber if hypoglycemia occurs because insulin dosage will need to be reduced.

Stress need to monitor blood glucose level often, especially before and after eating.

Tell patient to inject drug subcutaneously immediately before major meals using an insulin syringe to draw up dose and using the same technique as with insulin administration, including rotating sites. Or, if patient has been prescribed the Symlin Pen injector, show her how to use it. Advise patient to inject drug into her abdomen or thigh and not to use her arm as an injection site because absorption may be too variable.

Warn patient not to mix pramlintide and insulin together in the same syringe.

Warn patient that nausea is common with pramlintide; urge her to notify prescriber because dosage may need to be decreased.

Caution patient that if she misses a dose, she should skip the missed dose and continue with the next scheduled dose.

Instruct patient to keep unopened pramlintide vials in the refrigerator; vials that have been opened may be kept in the refrigerator or at room temperature.Vials should be discarded 28 days after opening.

Caution patient to avoid hazardous activities that require mental alertness until effects of pramlintide are known.

Reassure patient that pramlintide won’t alter her awareness of or her body’s response to insulin-induced hypoglycemia.

Alert patient that she’ll need close followup care, at least weekly until a target dose of pramlintide has been reached, she’s tolerating the drug well, and her blood glucose level is stable.

Instruct women of childbearing age to notify prescriber about planned, suspectpramlintide acetate 848 ed, or known pregnancy because drug therapy will need to be adjusted.

Explain that local injection site reactions, such as redness, swelling or itching, may occur but usually resolve in a few weeks.

Category

Chemical class: Thienopyridine
Therapeutic class: Platelet activation and aggregation inhibitor, antiplatelet

Pregnancy category: B

Indications

To reduce rate of thrombotic cardiovascular events in patients with acute coronary syndrome who will be managed with percutaneous coronary intervention because of unstable angina, non-ST-elevation MI, or ST-elevation MI
Adults. Initial: 60 mg as a loading dose and then 10 mg once daily. Maintenance: 10 mg once daily.
DOSAGE ADJUSTMENT For patients weighing less than 60 kg (132 lb), daily maintenance dosage may be reduced to 5 mg once daily. Route Onset Peak Duration P.O. 2 hr 30 min 7–10 days

Mechanism of Action

After forming active metabolite, irreversibly binds to ADP receptors on platelets to inhibit platelet activation and aggregation for the lifetime of the platelet, which is 7 to 10 days. Without platelet activation and aggregation, thrombus cannot form.

Contraindications

Active bleeding, history of transient ischemic attack or stroke, hypersensitivity to prasugrel or its components

Interactions

fibrinolytic agents, heparin, NSAIDs (chronic use),
warfarin: Increased risk of bleeding

Side Efect

CNS: Dizziness, fatigue, fever, headache, intracranial hemorrhage
CV: Atrial fibrillation, bradycardia, hypercholesterolemia, hyperlipidemia, hypertension, hypotension, peripheral edema
EENT: Epistaxis, retinal hemorrhage
GI: Diarrhea, GI or retroperitoneal hemorrhage, hepatic dysfunction, nausea
HEME: Anemia, leukopenia, mild to lifethreatening bleeding, severe thrombocytopenia, thrombotic thrombocytopenic purpura
MS: Back or limb pain
RESP: Cough, dyspnea, hemoptysis
SKIN: Subcutaneous hematoma, rash
Other: Allergic reaction, angioedema, malignancies, noncardiac chest pain

Cautions

Be aware that patient should be receiving daily aspirin therapy (75 mg or 325 mg) throughout prasugrel therapy.

Drug isn’t recommended for patients age 75 or older (except in high-risk situations such as the presence of diabetes or history of previous MI) or in patients who have active bleeding or a history of a transient ischemic attack or stroke. Monitor patients closely who have other risk factors for bleeding, which include a body weight less than 60 kg, a history of bleeding, or concurrent use of that increase risk of bleeding, such as warfarin, heparin, fibrinolytic therapy, or chronic use of NSAIDs.

Prasugrel shouldn’t be given to patients likely to undergo emergency coronary artery bypass graft (CABG) surgery because of increased bleeding risk. Drug should be discontinued at least 7 days before any surgery.
WARNING Monitor patient closely for bleeding because prasugrel can cause lifethreatening hemorrhage. Report hypotension in patients who have recently undergone coronary angiography, percutaneous coronary intervention, CABG surgery, or other surgical procedures while taking drug. In this setting, expect therapy to continue because stopping prasugrel, especially in first few weeks after acute coronary syndrome, increases the risk of adverse cardiovascular effects.

Because prasugrel inhibits platelet aggregation for the lifetime of the platelet, which is 7 to 10 days, withholding a dose prasugrel 849 P is unlikely help in managing a bleeding event or the risk of bleeding associated with an invasive procedure. Expect to administer exogenous platelets but only 6 hours after prasugrel loading dose or 4 hours after maintenance dose was given.

Monitor patient’s CBC regularly, as ordered, watching for evidence of thrombotic thrombocytopenic purpura, such as fever, neurologic abnormalities, renal dysfunction, and abnormal blood counts. Notify prescriber immediately because condition can be fatal. Expect to implement emergency treatment, such as plasmapheresis.

PATIENT SAFTY

Stress importance of taking prasugrel exactly as prescribed, without lapses in therapy, for drug to be effective and

Side Efect

to be reduced.

Instruct patient to take daily dose of aspirin as prescribed.

Discourage use of NSAIDs, including OTC products, during prasugrel therapy because of risk of bleeding.

Caution patient that bleeding may last longer than usual. Instruct him to report unusual bleeding or bruising.

Instruct patient to inform health care providers that he takes prasugrel.

Urge patient to take precautions against bleeding, such as using an electric shaver and a soft-bristled toothbrush.

Advise patient to avoid activities that could cause traumatic injury and bleeding.

Category

Chemical class: Mevinic acid derivative
Therapeutic class: Antihyperlipidemic

Pregnancy category: X

Indications

To prevent coronary and cardiovascular events in patients at risk, to treat hyperlipidemia
Adults. Initial: 10 to 40 mg daily at bedtime, increased every 4 wk, as needed. Maintenance: 10 to 80 mg at bedtime.
DOSAGE ADJUSTMENT For patients with significant renal or hepatic impairment, those taking immunosuppressants, and elderly patients, initial dosage reduced to 10 mg daily at bedtime. For elderly patients and those taking immunosuppressants, maintenance dosage usually limited to 20 mg daily. To treat pediatric heterozygous familial hypercholesterolemia Adolescents ages 14 to 18. 40 mg daily at bedtime. Children ages 8 to 14. 20 mg daily at bedtime.

Mechanism of Action

Inhibits cholesterol synthesis in liver by blocking the enzyme needed to convert hydroxymethylglutaryl-CoA (HMG-CoA) to mevalonate, a cholesterol precursor. When cholesterol synthesis is blocked, the liver also increases breakdown of LDL cholesterol.

Contraindications

Active hepatic disease or unexplained, persistent elevated liver function test results; breastfeeding; hypersensitivity to pravastatin or its components; pregnancy

Interactions

cholestyramine, colestipol: Decreased pravastatin bioavailability cyclosporine, erythromycin, gemfibrozil, immunosuppressants, niacin: Increased risk of rhabdomyolysis and acute renal failure oral anticoagulants: Increased bleeding or prolonged PT

Side Efect

CNS: Anxiety, depression, dizziness, fatigue, headache, nervousness, sleep disturbance
CV: Angina pectoris, chest pain
EENT: Blurred vision, diplopia, rhinitis
ENDO: Abnormal thyroid function
GI: Abdominal pain, constipation, diarrhea, elevated liver function test results, flatulence, heartburn, indigestion, nausea, pancreatitis, vomiting
GU: Dysuria, nocturia, urinary frequency
MS: Arthralgia, musculoskeletal cramps or pain, myalgia, myopathy, rhabdomyolysis
RESP: Cough, dyspnea, upper respiratory tract infection
SKIN: Rash
Other: Angioedema

Cautions

Use pravastatin cautiously in patients with renal or hepatic impairment and in elderly patients.

Monitor liver function test results before pravastatin therapy starts, before dosage increases, and periodically throughout therapy, as prescribed.

Give drug 1 hour before or 4 hours after giving cholestyramine or colestipol.

Report unexplained muscle aches or weakness and significant increases in CK level to prescriber because drug rarely causes rhabdomyolysis with acute renal failure caused by myoglobinuria. Expect to stop drug and provide supportive care.

Monitor patient’s BUN and serum creatinine levels periodically for abnormal elevations.

Monitor blood lipoprotein level, as indicated, to evaluate response to therapy.

PATIENT SAFTY

Instruct patient to take drug at bedtime, without regard to meals.

Advise patient to notify prescriber at once about muscle pain, tenderness, weakness, and other evidence of myopathy.

Urge woman of childbearing age to use a reliable method of contraception during pravastatin therapy and to notify prescriber at once if she becomes pregnant or thinks she may be pregnant.

Instruct patient not to stop taking pravastatin without consulting prescriber, even when cholesterol level returns to normal.

Category

Chemical class: Quinazoline derivative
Therapeutic class: Antihypertensive

Pregnancy category: C

Indications

To manage hypertension
Adults. Initial: 1 mg b.i.d. or t.i.d. Maintenance: 6 to 15 mg daily in divided doses b.i.d. or t.i.d. Maximum: 40 mg daily. Children. Initial: 50 to 400 mcg/kg daily in divided doses b.i.d. or t.i.d. Maximum: 7 mg/dose, 15 mg daily.
Adults. Initial: 0.5 mg b.i.d. or t.i.d. for at least 3 days; then increased to 1 mg b.i.d. or t.i.d., if tolerated, for an additional 3 days. Subsequent dosages adjusted gradually, as needed and tolerated. Maintenance: 6 to 15 mg daily in divided doses b.i.d. or t.i.d. Maximum: 40 mg daily. Children. Initial: 50 to 400 mcg/kg daily in divided doses b.i.d. or t.i.d. Maximum: 7 mg/dose, 15 mg daily.
DOSAGE ADJUSTMENT For elderly patients and those with renal impairment, initial dosage possibly reduced to 1 mg once to twice daily. Route Onset Peak Duration P.O. 0.5–1.5 hr 2–4 hr* 7–10 hr

Mechanism of Action

Selectively and competitively inhibits alpha1-adrenergic receptors. This action promotes peripheral arterial and venous dilation and reduces peripheral vascular resistance, thereby lowering blood pressure.

Contraindications

Hypersensitivity to prazosin, other quinazolines, or their components

Interactions

antihypertensives, beta blockers, diuretics, phosphodiesterase-5 inhibitors: Increased risk of hypotension and syncope dopamine: Antagonized peripheral vasoconstrictive effect of dopamine (high doses) ephedrine: Decreased vasopressor response to ephedrine epinephrine: Possibly severe hypotension and tachycardia metaraminol: Decreased vasopressor effect of metaraminol methoxamine, phenylephrine: Possibly decreased vasopressor effect and shortened duration of action of these NSAIDs, sympathomimetics: Decreased effectiveness of prazosin

Side Efect

CNS: Asthenia, dizziness, drowsiness, * For a single dose; 3 to 4 wk for multiple doses. fatigue, headache, insomnia, malaise, nervousness, syncope
CV: Angina, bradycardia, edema, orthostatic hypotension, palpitations, vasculitis
EENT: Dry mouth, eye pain
ENDO: Gynecomastia
GI: Nausea
GU: Urinary frequency,urinary incontinence
SKIN: Urticaria
Other: Hypersensitivity reaction

Cautions

Use prazosin cautiously in patients with renal impairment because of increased sensitivity to prazosin’s effects; in those with angina pectoris because drug may induce or aggravate angina; in those with narcolepsy because prazosin may worsen cataplexy; and in elderly patients because they’re at increased risk for drug-induced hypotension.

Monitor blood pressure regularly to evaluate effectiveness of therapy.

PATIENT SAFTY

Instruct patient who is starting prazosin to take drug at bedtime to minimize effects of first-dose hypotension.

Stress need to take drug even if feeling well.

Advise patient to avoid drinking alcohol, standing for long periods, and exercising in hot weather because these activities increase risk of orthostatic hypotension.

Suggest rising slowly from lying or sitting position to minimize orthostatic hypotension.

Urge patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to notify prescriber immediately about

Side Efect

, especially dizziness and fainting.

Instruct patient not to take any , including OTC forms, without consulting prescriber, to avoid serious interactions.

Category

Chemical class: Glucocorticoid
Therapeutic class: Anti-inflammatory, immunosuppressant

Pregnancy category: C

Indications

To treat adrenal insufficiency and acute and chronic inflammatory and immunosuppressive disorders SYRUP,(PREDNISOLONE);
, (PREDNISOLONE SODIUM PHOSPHATE); ORAL SUSPENSION(PREDNISOLONE ACETATE) Adults and adolescents. 5 to 60 mg daily or in divided doses. Maximum: 250 mg daily.
I.M.INJECTION(PREDNISOLONE ACETATE) Adults and adolescents. 4 to 60 mg daily. INTRA-ARTICULAR, INTRALESIONAL, OR SOFT-TISSUE INJECTION(PREDNISOLONE ACETATE, PREDNISOLONE TEBUTATE) Adults and adolescents. 4 to 100 mg of prednisolone acetate, repeated as needed, or 4 to 40 mg of prednisolone tebutate, repeated every 1 to 3 wk, as needed. To treat adrenocortical insufficiency in children SYRUP,(PREDNISOLONE);
, (PREDNISOLONE SODIUM PHOSPHATE); ORAL SUSPENSION(PREDNISOLONE ACETATE) Children. 0.14 mg/kg daily in divided doses t.i.d.
I.M.INJECTION(PREDNISOLONE ACETATE) Children. 0.14 mg/kg over a 24-hr period in divided doses t.i.d. every third day. To treat acute exacerbations of multiple sclerosis SYRUP,(PREDNISOLONE);
, prednisolone 852 (PREDNISOLONE SODIUM PHOSPHATE); ORAL SUSPENSION(PREDNISOLONE ACETATE)
Adults. 200 mg daily for 1 wk, followed by 80 mg every other day for 1 mo. Route Onset Peak Duration P.O.* Unknown 1–2 hr 1.25–1.5 days I.M. Slow Unknown Unknown Intra1– 2 days Unknown 1–3 wk articular, intralesional, soft-tissue injection

Mechanism of Action

Binds to intracellular glucocorticoid receptors and suppresses inflammatory and immune responses by:

inhibiting neutrophil and monocyte accumulation at inflammation site and suppressing their phagocytic and bactericidal activity

stabilizing lysosomal membranes

suppressing antigen response of macrophages and helper T cells

inhibiting synthesis of inflammatory response mediators, such as cytokines, interleukins, and prostaglandins.

Contraindications

Hypersensitivity to prednisolone or its components, idiopathic thrombocytopenic purpura (I.M. form), systemic fungal infection

Interactions

acetaminophen: Possibly hepatotoxicity (long-term use or high acetaminophen doses) acetazolamide: Possibly hypernatremia or edema amphotericin B (parenteral): Possibly severe hypokalemia anabolic steroids, androgens: Possibly edema and severe acne anticholinergics: Increased intraocular pressure asparaginase: Increased hyperglycemic effect of asparaginase, possibly neuropathy and disturbances in erythropoiesis carbonic anhydrase inhibitors: Possibly hypocalcemia, hypokalemia, and osteoporosis digoxin: Possibly arrhythmias and digitalis toxicity from hypokalemia diuretics: Possibly decreased natriuretic and diuretic effects of diuretics, severe hypokalemia (with potassium-depleting diuretics) ephedrine: Increased metabolic clearance of prednisolone estrogens, oral contraceptives: Decreased clearance, increased elimination half-life, and increased therapeutic and toxic effects of prednisolone folic acid: Increased folic acid requirements (with long-term prednisolone use) heparin, oral anticoagulants, streptokinase, urokinase: Possibly decreased anticoagulant effect and increased risk of GI ulceration and bleeding immunosuppressants: Increased risk of infection, lymphomas, and other lymphoproliferative disorders isoniazid: Decreased blood isoniazid level
mexiletine: Possibly accelerated metabolism and decreased blood level of mexiletine neuromuscular blockers: Increased neuromuscular blockade
NSAIDs: Increased risk of GI ulceration and bleeding, possibly added therapeutic effect when NSAIDs are used to treat arthritis potassium supplements: Decreased effectiveness of both rifampin, other hepatic enzyme inducers: Decreased prednisolone effect ritodrine: Increased risk of pulmonary edema in pregnant women salicylates: Possibly decreased blood salicylate level, increased risk of GI ulceration and bleeding sodium-containing : Possibly edema and hypertension somatrem, somatropin: Inhibited growth response to somatrem or somatropin streptozocin: Increased risk of hyperglycemia toxoids, vaccines: Possibly loss of antibody response, increased risk of neurologic complications tricyclic antidepressants: Possibly worsened adverse psychiatric effects of prednisolone troleandomycin: Increased therapeutic and toxic effects of prednisolone * Prednisolone Prednisolone acetate Prednisolone tebutate sodium-containing : Increased risk of edema and hypertension
alcohol use: Increased risk of GI ulceration and bleeding

Side Efect

CNS: Euphoria, headache, insomnia, nervousness, psychosis, restlessness, seizures, vertigo
CV: Edema, heart failure, hypertension
EENT: Cataracts, exophthalmos, glaucoma, increased ocular pressure
ENDO: Adrenal insufficiency, Cushing’s syndrome, growth suppression in children, hyperglycemia
GI: Anorexia, GI bleeding and ulceration, increased appetite, indigestion, intestinal perforation, nausea, pancreatitis, vomiting
GU: Menstrual irregularities
MS: Avascular necrosis of joints, bone fractures, muscle atrophy or weakness, myalgia, osteoporosis, tendon rupture (local injection only)
SKIN: Acne; cutaneous or subcutaneous atrophy (with frequent repository injections); diaphoresis; ecchymosis; flushing; petechiae; striae; thin, fragile skin
Other: Delayed wound healing, hypernatremia, hypokalemia, injection site scarring, negative nitrogen balance

Cautions

WARNING Avoid using prednisolone in patients with a history of active tuberculosis because drug can reactivate the disease.

Give once-daily doses in the morning to mirror body’s normal cortisol secretion.

Inspect injectable form for particulates and discoloration before administering.

For I.M. injection, shake suspension well before withdrawing. Keep in mind that I.M. injections are contraindicated in patients with idiopathic thrombocytopenic purpura.

For intra-articular injection, attach a 20G to 24G needle to empty syringe, using aseptic technique, so prescriber can remove a few drops of synovial fluid to confirm that needle is in the joint. The aspirating syringe is then exchanged with a prenisolone-filled syringe to inject drug into joint.

Because prednisolone can produce many

Side Efect

, assess patient regularly for evidence of such reactions, including heart failure and hypertension. Also monitor patient’s intake, output, and daily weight.

Monitor growth pattern in children; prednisolone may retard bone growth.

Prolonged use may cause hypothalamicpituitary-adrenal suppression.
WARNING Withdraw drug gradually, as ordered, if therapy lasts longer than 2 weeks. Stopping abruptly may cause acute adrenal insufficiency or, possibly, death.

Be aware that patient may be at risk for emotional instability or psychic disturbance while taking prednisolone, especially if predisposed to them or taking high doses.

PATIENT SAFTY

Instruct patient to take oral prednisolone with food to decrease stomach upset and to take once-daily dose in the morning.

Stress nweed to take drug exactly as prescribed; taking too much increases risk of serious

Side Efect

.

Instruct patient taking orally disintegrating tablets to remove tablet from blister pack only when ready to take drug and to place tablet on tongue. Warn her not to split, cut, or break tablets.

Caution patient not to discontinue drug abruptly.

Urge patient to avoid alcohol during therapy because of increased risk of GI ulcers and bleeding.

Urge patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to avoid people with contagious infections because drug has an immunosuppressant effect. Urge her to notify prescriber immediately about exposure to measles or chickenpox.

Caution against receiving vaccinations or other immunizations and coming in contact with people who have recently received oral poliovirus vaccine.

Teach patient about potential side effects of prednisolone therapy, including restlessness, mood swings, nervousness, and delayed wound healing.

Instruct patient to notify prescriber immediately about joint pain, swelling, tarry stools, and visual disturbances. Also instruct her to report signs of infection or prednisolone 854 injury for up to 12 months after therapy.

Advise patient to restrict joint use after intra-articular injection and to obtain activity guidelines from prescriber.

Instruct diabetic patient to check her blood glucose level often because prednisolone may cause hyperglycemia.

Advise patient to comply with follow-up visits to assess drug’s effectiveness and detect

Side Efect

.

Urge patient to carry medical identification revealing prednisolone therapy.

Category

Chemical class: Glucocorticoid
Therapeutic class: Anti-inflammatory, immunosuppressant

Pregnancy category: Not rated

Indications

To treat adrenal insufficiency and acute and chronic inflammatory and immunosuppressive disorders

ORALL

, SYRUP, Adults and adolescents. 5 to 60 mg daily as a single dose or in divided doses. Maximum: 250 mg daily. To treat adrenogenital syndrome

ORALL

, SYRUP, Adults and adolescents. 5 to 10 mg daily. Children. 5 mg/m2daily in divided doses b.i.d. To treat acute exacerbations of multiple sclerosis

ORALL

, SYRUP,
Adults. 200 mg daily for 1 wk, then 80 mg every other day for 1 mo. Maximum: 250 mg daily. To treat nephrosis in children

ORALL

, SYRUP, Children age 10 and over. 20 mg q.i.d. Children ages 4 to 10. 15 mg q.i.d. Children ages 18 months to 4 years. 7.5 to 10 mg q.i.d. To treat rheumatic carditis, leukemia, and tumors in children

ORALL

, SYRUP, Children. 0.5 mg/kg q.i.d. for 2 to 3 wk; then 0.375 mg/kg q.i.d. for 4 to 6 wk. As adjunct to treat tuberculosis in children (with concurrent antitubercular therapy)

ORALL

, SYRUP, Children. 0.5 mg/kg q.i.d. for 2 mo. Route Onset Peak Duration P.O. Rapid 1–2 hr 1.25–1.5 days

Mechanism of Action

Binds to intracellular glucocorticoid receptors and suppresses inflammatory and immune responses by:

inhibiting neutrophil and monocyte accumulation at inflammation site and suppressing their phagocytic and bactericidal activity

stabilizing lysosomal membranes

suppressing antigen response of macrophages and helper T cells

inhibiting synthesis of inflammatory response mediators, such as cytokines, interleukins, and prostaglandins.

Contraindications

Hypersensitivity to prednisone or its components, systemic fungal infection

Interactions

acetaminophen: Possibly hepatotoxicity (long-term use or high acetaminophen doses) acetazolamide sodium: Possibly hypernatremia or edema amphotericin B (parenteral): Possibly severe hypokalemia anabolic steroids, androgens: Possibly edema and severe acne antacids: Decreased absorption of prednisone (with long-term use) anticholinergics: Increased intraocular pressure asparaginase: Increased hyperglycemic effect of asparaginase, possibly neuropathy and disturbances in erythropoiesis carbonic anhydrase inhibitors: Possibly hypocalcemia, hypokalemia, and osteoporosis digoxin: Possibly arrhythmias and digitalis toxicity from hypokalemia diuretics: Possibly decreased natriuretic and diuretic effects of diuretics, severe hypokalemia (with potassium-depleting diuretics) ephedrine: Increased metabolic clearance of prednisone estrogens, oral contraceptives: Decreased clearance, increased elimination half-life, and increased therapeutic and toxic effects of prednisone folic acid: Increased folic acid requirements (with long-term prednisone use) heparin, oral anticoagulants, streptokinase, urokinase: Possibly decreased anticoagulant effect and increased risk of GI ulceration and bleeding immunosuppressants: Increased risk of infection, lymphomas, and other lymphoproliferative disorders isoniazid: Decreased blood isoniazid level
mexiletine: Possibly accelerated metabolism and decreased blood level of mexiletine neuromuscular blockers: Increased neuromuscular blockade
NSAIDs: Increased risk of GI ulceration and bleeding, possibly added therapeutic effect when NSAIDs are used to treat arthritis potassium supplements: Decreased effectiveness of both ritodrine: Increased risk of pulmonary edema in pregnant women salicylates: Possibly decreased blood salicylate level, increased risk of GI ulceration and bleeding sodium-containing : Possibly edema and hypertension somatrem, somatropin: Inhibited growth response to somatrem or somatropin streptozocin: Increased risk of hyperglycemia toxoids, vaccines: Possibly loss of antibody response, increased risk of neurologic complications tricyclic antidepressants: Possibly exacerbated adverse psychiatric effects of prednisone troleandomycin: Increased therapeutic and toxic effects of prednisone sodium-containing : Increased risk of edema and hypertension
alcohol use: Increased risk of GI ulceration and bleeding

Side Efect

CNS: Euphoria, headache, insomnia, nervousness, psychosis, restlessness, seizures, vertigo
CV: Edema, heart failure, hypertension
EENT: Cataracts, exophthalmos, glaucoma, increased ocular pressure
ENDO: Adrenal insufficiency, Cushing’s syndrome, growth suppression in children, hyperglycemia
GI: Anorexia, GI bleeding and ulceration, increased appetite, indigestion, intestinal perforation, nausea, pancreatitis, vomiting
GU: Menstrual irregularities
MS: Avascular necrosis of joints, bone fractures, muscle atrophy or weakness, myalgia, osteoporosis
SKIN: Acne; diaphoresis; ecchymosis; flushing; petechiae; striae; thin, fragile skin
Other: Delayed wound healing, hypernatremia, hypokalemia, negative nitrogen balance

Cautions

Administer once-daily doses of prednisone in the morning to match body’s normal cortisol secretion schedule.

Because prednisone can produce many

Side Efect

, assess regularly for signs and symptoms of such reactions as heart failure and hypertension. Also monitor fluid intake and output and daily weight.

Monitor growth pattern in children. Prednisone may retard bone growth.

Be aware that prolonged use of prednisone may cause hypothalamic-pituitary-adrenal suppression.
WARNING Withdraw prednisone gradually, as ordered, if therapy lasts longer than 2 weeks. Stopping abruptly may cause acute adrenal insufficiency and, possibly, death.

PATIENT SAFTY

Instruct patient to take prednisone with food to decrease GI distress and to take once-daily dose in the morning.

Stress importance of taking drug exactly as prescribed; taking more than prescribed increases risk of serious

Side Efect

.

Caution patient not to stop drug abruptly.

Urge patient to avoid alcohol during therapy because of increased risk of GI ulcers and bleeding.

Urge patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to avoid people with contagious infections because drug has an immunosuppressant effect. Urge her to prednisone 856 notify prescriber immediately about possible exposure to measles or chickenpox.

Caution against receiving vaccinations or other immunizations and coming in contact with people who have recently received oral poliovirus vaccine.

Instruct patient to notify prescriber immediately about joint pain, swelling, tarry stools, and visual disturbances. Also instruct her to report signs of infection or injury for up to 12 months after therapy.

Instruct diabetic patient to check blood glucose level often because prednisone may cause hyperglycemia.

Advise patient to comply with follow-up visits to assess drug effectiveness and detect

Side Efect

.

Urge patient to carry medical identification revealing prednisone therapy.

Category

Chemical class: Structural derivative of gamma-aminobutyric acid (GABA)
Therapeutic class: Analgesic, anticonvulsant

Pregnancy category: C

Indications

To relieve neuropathic pain associated with diabetic peripheral neuropathy
Adults. Initial: 50 mg t.i.d., increased to 100 mg t.i.d. within 1 wk as needed. To relieve postherpetic neuralgia; as adjunct therapy to manage partial onset seizures
Adults. Initial: 75 mg b.i.d. or 50 mg t.i.d., increased to 150 mg b.i.d. or 100 mg t.i.d. within 1 week as needed. Then increased to 300 mg b.i.d. or 200 mg t.i.d. in 2 to 4 weeks as needed. To manage fibromyalgia
Adults. Initial: 75 mg b.i.d., increased to 150 mg b.i.d. in 1 wk, as needed, and then to 225 mg b.i.d. in 1 wk as needed. Maximum: 450 mg daily.
DOSAGE ADJUSTMENT If creatinine clearance is 30 to 60 ml/min/1.73 m2, daily dosage reduced by 50%. If clearance is 15 to 30 ml/ min/1.73 m2, daily dosage reduced by 75% and frequency reduced to once or twice daily. If clearance is less than 15 ml/min/ 1.73 m2, daily dosage reduced to as low as 25 mg daily. If patient is having hemodialysis, daily dosage is reduced and supplemental dose given immediately after every 4hour hemodialysis session as follows: If reduced daily dosage is 25 mg daily, give supplemental dose of 25 to 50 mg. If reduced daily dosage is 25 to 50 mg daily, give supplemental dose of 50 to 75 mg. If reduced daily dosage is 75 mg, give supplemental dose of 100 to 150 mg. Route Onset Peak Duration P.O. Unknown 1.5 hr Unknown

Mechanism of Action

Binds to alpha2-delta site, an auxiliary subunit of voltage calcium channels, in CNS tissue where it may reduce calcium-dependent release of several neurotransmitters, possibly by modulating calcium channel function. With fewer neurotransmitters, pain sensation and seizure activity decline.

Contraindications

Hypersenstivity to pregabalin or its components

Interactions

ACE inhibitors: Increased risk of pregabalininduced angioedema
CNS depressants: Additive CNS effects such as somnolence lorazepam, oxycodone: Additive effects on cognitive and gross motor function thiazolidinedione antidiabetics: Possibly increased risk of peripheral edema and weight gain
alcohol use: Additive effects on cognitive and gross motor function

Side Efect

CNS: Abnormal gait, amnesia, anxiety, asthenia, ataxia, balance disorder, confusion, depression, difficulty concentrating, dizziness, euphoria, extrapyramidal syndrome, fatigue, fever, headache, hypertonia, hypesthesia, incoordination, intracranial hypertension, myoclonus, nervousness, neuropathy, paresthesia, psychotic deprespregabalin 857 P sion, schizophrenic reaction, somnolence, stupor, suicidal ideation, tremor, twitching, vertigo
CV: Chest pain, heart failure, peripheral edema, ventricular fibrillation
EENT: Amblyopia, blurred vision, conjunctivitis, decreased visual acuity, diplopia, dry mouth, nystagmus, otitis media, sinusitis, tinnitus, visual field defect
ENDO: Hypoglycemia
GI: Abdominal distention or pain, constipation, diarrhea, flatulence, gastroenteritis, GI hemorrhage, increased appetite, nausea, vomiting
GU: Acute renal failure, anorgasmia, decreased libido, glomerulitis, impotence, nephritis, urinary frequency, urinary incontinence, urine retention
HEME: Decreased platelet count, leukopenia, thrombocytopenia
MS: Arthralgia, back pain, elevated creatine kinase level, leg or muscle cramps, myalgia, myasthenia
RESP: Apnea, dyspnea
SKIN: Ecchymosis, exfoliative dermatitis, pruritus
Other: Anaphylaxis, angioedema, facial edema, hypersensitivity reaction, StevensJohnson syndrome, weight gain

Cautions

Pregabalin therapy should be stopped gradually over at least 1 week to decrease risk of seizure activity and avoid unpleasant symptoms such as diarrhea, headache, insomnia, and nausea.

If patient has evidence of hypersensitivity (red skin, urticaria, rash, dyspnea, facial swelling, wheezing), stop drug at once, notify prescriber, and give supportive care.

Monitor patient closely for adverse reactions. Notify prescriber if significant

Side Efect

persist.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

PATIENT SAFTY

Warn against stopping pregabalin abruptly.

Urge patient to avoid hazardous activities until she knows how drug affects her.

Instruct patient to notify prescriber if she has changes in vision or unexplained muscle pain, tenderness, or weakness, especially if these muscle symptoms are accompanied by malaise or fever.

Alert patient that drug may cause edema and weight gain.

If patient also takes a thiazolidinedione antidiabetic, tell her these effects may be intensified. If significant, tell patient to notify prescriber.

Inform male patient who plans to father a child that drug could impair his fertility.

Instruct diabetic patients to inspect their skin while taking pregabalin.

Urge caregivers to watch patient closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes and to report concerns at once to prescriber.

Category

Chemical class: Prodrug of phenobarbital
Therapeutic class: Anticonvulsant

Pregnancy category: Not rated

Indications

To manage generalized tonic-clonic seizures, nocturnal myoclonic seizures, complex partial seizures, and simple partial seizures caused by epilepsy CHEWABLE , ORAL SUSPENSION, Adults and children age 8 and over. Initial: 100 or 125 mg at bedtime for first 3 days; then increased to 100 or 125 mg b.i.d. for next 3 days, followed by 100 or 125 mg t.i.d. for next 3 days. On 10th day, begin maintenance dosage as prescribed. Maintenance: 250 mg t.i.d. or q.i.d., adjusted as needed. Maximum: 2 g daily. Children up to age 8. Initial: 50 mg at bedtime for first 3 days; then increased to 50 mg b.i.d. for next 3 days, followed by increase to 100 mg b.i.d. for next 3 days. On 10th day, begin maintenance dosage. Maintenance: 125 to 250 mg t.i.d., adjusted as needed. primidone 858

Mechanism of Action

Prevents seizures by decreasing excitability of neurons and increasing motor cortex’s threshold of electrical stimulation.

Contraindications

Hypersensitivity to primidone, phenobarbital, or their components; porphyria

Interactions

acetaminophen: Decreased acetaminophen effectiveness, increased risk of hepatotoxicity adrenocorticoids, chloramphenicol, cyclosporine, dacarbazine, disopyramide, doxycycline, levothyroxine, metronidazole, mexiletine, oral anticoagulants, oral contraceptives (estrogencontaining), quinidine, tricyclic antidepressants: Decreased effectiveness of these amphetamines: Possibly delayed absorption of primidone anticonvulsants: Possibly altered pattern of seizures carbamazepine: Decreased effectiveness of primidone carbonic anhydrase inhibitors: Increased risk of osteopenia
CNS depressants: Possibly enhanced CNS and respiratory depressant effects of both cyclophosphamide: Reduced half-life and increased leukopenic activity of cyclophosphamide enflurane, halothane,
methoxyflurane: Increased risk of hepatotoxicity; increased risk of nephrotoxicity (with methoxyflurane) fenoprofen: Decreased elimination half-life of fenoprofen folic acid: Increased folic acid requirements griseofulvin: Decreased antifungal effects of griseofulvin guanadrel, guanethidine: Possibly aggravated orthostatic hypotension haloperidol, loxapine, maprotiline, molindone, phenothiazines,
thioxanthenes: Possibly lowered seizure threshold and increased CNS depression leucovorin: Possibly decreased anticonvulsant effects of primidone (with large doses)
MAO inhibitors: Possibly prolonged primidone effects and altered seizure pattern
methylphenidate: Possibly increased blood primidone level, resulting in toxicity phenobarbital: Increased sedative effects of either drug, possibly altered seizure pattern phenylbutazone: Decreased primidone effectiveness, increased metabolism and decreased half-life of phenylbutazone
rifampin: Decreased blood primidone level
valproic acid: Increased blood primidone level, leading to increased CNS depression and neurotoxicity; decreased valproic acid half-life and increased hepatotoxicity risk
vitamin D: Decreased effects of vitamin D xanthines: Increased metabolism and clearance of xanthines (except dyphylline)
alcohol use: Possibly increased CNS and respiratory depressant effects of primidone

Side Efect

CNS: Ataxia, confusion, dizziness, drowsiness, excitement, mental changes, mood changes, restlessness
EENT: Diplopia, nystagmus
GI: Anorexia, nausea, vomiting
GU: Impotence
RESP: Dyspnea
Other: Folic acid deficiency

Cautions

Monitor blood levels of primidone and phenobarbital (its active metabolite), as ordered, to determine therapeutic level or detect toxic levels.

Anticipate that drug may cause confusion, excitement, or mood changes in elderly patients and children.

Assess for signs of folic acid deficiency: mental dysfunction, neuropathy, tiredness, and weakness.

PATIENT SAFTY

Instruct patient to crush primidone tablets and mix with food or fluids, as needed.

Advise patient taking oral suspension to shake bottle well and measure doses with a calibrated device.

Suggest that patient take drug with meals to minimize adverse GI reactions.

Urge patient not to stop taking primidone abruptly because doing so can precipitate seizures.

Caution patient about possible decreased alertness.

Advise her to avoid hazardous activities until drug’s CNS effects are known.

Urge patient to avoid consuming alcohol and other CNS depressants during primidone therapy.

Category

Chemical class: Sulfonamide derivative
Therapeutic class: Antibiotic adjunct, antigout, uricosuric

Pregnancy category: Not rated

Indications

To treat chronic gouty arthritis and hyperuricemia due to chronic gout Adults and adolescents. Initial: 250 mg b.i.d. for 1 wk; then increased to maintenance dosage. Maintenance: 500 mg b.i.d.; if not effective or 24-hr uric acid excretion isn’t greater than 700 mg, dosage increased by 500 mg/day every 4 wk, as needed and prescribed, up to a maximum of 3 g daily. If no acute attacks of gout occur over next 6 mo and serum uric acid level is within normal limits, dosage decreased, as prescribed, by 500 mg every 6 mo until lowest effective maintenance dose is reached. Maximum: 3 g daily.
DOSAGE ADJUSTMENT Dosage possibly increased for patients with mild renal dysfunction, except for elderly patients, who require a dosage reduction. As adjunct to antibiotic therapy with penicillins and some cephalosporins Adults,adolescents age 14 and over,and children weighing more than 50 kg (110 lb). 500 mg q.i.d.; if given with I.V. or I.M. antibiotic, administer at least 30 min before antibiotic. Children ages 2 to 14 weighing up to 50 kg. 25 mg/kg as single dose, then 10 mg/kg q.i.d.; if given with I.V. or I.M. antibiotic, give at least 30 min before antibiotic. As adjunct to treat sexually transmitted diseases Adults and adolescents. 1 g as single dose, given with appropriate antibiotic. As adjunct to treat pediatric gonorrhea Postpubertal children and children weighing more than 45 kg (99 lb). 1 g as single dose, given with appropriate antibiotic. As adjunct to treat neurosyphilis Adults and adolescents. 500 mg q.i.d. with 1 daily dose (2.4 million units) of penicillin G procaine for 10 to 14 days. Route Onset Peak Duration P.O. Unknown 30 min* 8 hr

Mechanism of Action

Increases urinary excretion of uric acid and lowers serum uric acid level, which may prevent or resolve urate deposits, tophus formation, and joint changes. Eventually, incidence of acute gout attacks decreases. Probenecid also inhibits renal excretion of penicillins and some cephalosporins, thereby increasing their serum concentration and prolonging their duration of action.

Contraindications

Age less than 2 years, blood dyscrasias, hypersensitivity to probenecid or its components, renal calculi (urate)

Interactions

acyclovir: Decreased renal tubular secretion of acyclovir allopurinol: Additive antihyperuricemic effects aminosalicylate sodium, cephalosporins, ciprofloxacin, clofibrate, dapsone, ganciclovir, imipenem, methotrexate, nitrofurantoin, norfloxacin, penicillins: Increased and possibly prolonged blood levels of these , increased risk of toxicity antineoplastics (rapidly cytolytic): Possibly uric acid nephropathy diazoxide, mecamylamine, pyrazinamide: Increased risk of hyperuricemia, decreased probenecid effectiveness dyphylline: Increased half-life of dyphylline furosemide: Increased blood furosemide level heparin: Increased and prolonged anticoagulant effect indomethacin, ketoprofen, other
NSAIDs: Possibly increased adverse effects lorazepam, oxazepam, temazepam: Increased * For renal clearance of uric acid; 2 hr for effect on blood antibiotic level. For effect on blood antibiotic level; unknown for renal clearance of uric acid. effects of these , possibly excessive sedation
riboflavin: Decreased GI absorption of riboflavin rifampin, sulfonamides: Increased blood levels of these and, possibly, toxicity salicylates: Decreased uricosuric effects of probenecid sodium benzoate and sodium phenylacetate: Decreased renal elimination of these sulfonylureas: Increased sulfonylurea halflife thiopental: Prolonged thiopental effect zidovudine: Increased risk of zidovudine toxicity
alcohol use: Increased risk of hyperuricemia, decreased probenecid effectiveness

Side Efect

CNS: Dizziness, headache
EENT: Sore gums
GI: Anorexia, nausea, vomiting
GU: Hematuria, renal calculi (urate), renal colic, urinary frequency
MS: Costovertebral pain; joint pain, redness, and swelling
SKIN: Facial flushing, pruritus, rash, urticaria

Cautions

Be aware that probenecid therapy shouldn’t start until acute gout attack has subsided. If acute attack starts during therapy, continue therapy as prescribed.

Use drug cautiously in patients with peptic ulcer disease.

Expect to give sodium bicarbonate (3 to 7.5 g daily) or potassium citrate (7.5 g daily), as prescribed, to keep urine alkaline and prevent renal calculus formation.

Monitor CBC, serum uric acid level, and liver and renal function test results during therapy.

Closely monitor patients receiving intermittent therapy because they’re more likely to develop allergic reactions.

Check blood glucose level often in diabetic patient who takes a sulfonylurea because of the risk of drug interactions.

PATIENT SAFTY

Advise patient to take probenecid with meals to minimize GI distress.

Encourage patient to increase fluid intake (up to 3 L daily, if not contraindicated) to help prevent renal calculus formation.

Instruct patient to notify prescriber immediately if she has signs of an acute gout attack (joint pain, swelling, and redness) or of renal calculi (flank pain and blood in urine).

Caution patient against taking salicylates while taking probenecid. Instead, advise acetaminophen to treat mild pain or fever.

Category

Chemical class: Ethyl benzamide monohydrochloride
Therapeutic class: Antiarrhythmic

Pregnancy category: C

Indications

To treat life-threatening ventricular arrhythmias ,
Adults. 50 mg/kg daily in 8 divided doses (every 3 hr), adjusted as needed and tolerated. Maximum: 6 g daily (maintenance). Children. 12.5 mg/kg q.i.d.
Adults. Maintenance: 50 mg/kg daily in divided doses q.i.d. (every 6 hr), adjusted as needed and tolerated. Maximum: 6 g daily (maintenance).

IV

OR INJECTION
Adults. Initial: 100 mg diluted in D5W and given at no more than 50 mg/min. Repeated every 5 min until arrhythmia is controlled or maximum total dose of 1 g is reached. Or, 10 to 15 mg/kg I.V. bolus given at 25 to 50 mg/min. Maintenance: 1 to 4 mg/min by continuous infusion.
I.M.INJECTION
Adults. 50 mg/kg daily in divided doses every 3 to 6 hr. To treat ventricular extrasystoles and arrhythmias associated with anesthesia and surgery

IV

OR INJECTION
Adults. Initial: 100 mg diluted in D5W and given at no more than 50 mg/min. Dosage repeated every 5 min until arrhythmia is controlled or maximum total dose of 1 g is reached. Or, 10 to 15 mg/kg I.V. bolus given at 25 to 50 mg/min. Maintenance: 1 to 4 mg/min by continuous infusion.
I.M.INJECTION
Adults. 100 to 500 mg every 3 to 6 hr.
DOSAGE ADJUSTMENT For elderly patients or those with cardiac or hepatic insufficiency, dosage possibly reduced or dosing intervals increased. For patients with creatinine clearance less than 50 ml/min/1.73 m2, initial dosage reduced to 1 to 2 mg/min. Route Onset Peak Duration P.O. Unknown Unknown 60– 90 min P.O. Unknown 60–90 Unknown () min I.V. Unknown Immediate Unknown I.M. 10–30 min 15–60 min Unknown

Mechanism of Action

Prolongs recovery period after myocardial repolarization by inhibiting sodium influx through myocardial cell membranes. This action prolongs refractory period, causing myocardial automaticity, excitability, and conduction velocity to decline.

Contraindications

Complete heart block, hypersensitivity to procainamide or its components, systemic lupus erythematosus, torsades de pointes

Interactions

antiarrhythmics: Additive cardiac effects anticholinergics, antidyskinetics, antihistamines: Possibly intensified atropine-like adverse effects, increased risk of ileus antihypertensives: Additive hypotensive effects antimyasthenics: Possibly antagonized effect of antimyasthenic on skeletal muscle bethanechol: Possibly antagonized cholinergic effect of bethanechol bone marrow depressants: Possibly increased leukopenic or thrombocytopenic effects bretylium: Possibly decreased inotropic effect of bretylium and enhanced hypotension neuromuscular blockers: Possibly increased or prolonged neuromuscular blockade pimozide: Possibly prolonged QT interval, leading to life-threatening arrhythmias

Side Efect

CNS: Chills, disorientation, dizziness, lightheadedness
CV: Heart block (second-degree), hypotension, pericarditis, prolonged QT interval, tachycardia
EENT: Bitter taste
GI: Abdominal distress, anorexia, diarrhea, nausea, vomiting
HEME: Agranulocytosis, neutropenia, thrombocytopenia
MS: Arthralgia, myalgia
RESP: Pleural effusion
SKIN: Pruritus, rash
Other: Drug-induced fever

Cautions

Place patient in a supine position before giving procainamide I.M. or I.V. to minimize hypotensive effects. Monitor blood pressure often and ECG tracings continuously during administration and for 30 minutes afterward.

Inspect parenteral solution for particles and discoloration before giving drug; discard if particles are present or solution is darker than light amber.

When possible, give drug by I.V. infusion or injection, as prescribed, rather than by I.M. injection.

If drug is to be given I.M. and patient’s platelet count is below 50,000/mm3, notify prescriber at once because patient may develop bleeding, bruising, or hematomas from procainamide-induced bone marrow suppression and thrombocytopenia. Expect to give procainamide I.V.

For I.V. injection, dilute procainamide with D5W according to manufacturer’s instructions before administration.

For I.V. infusion, dilute 200 to 1,000 mg of procainamide to a concentration of 2 or 4 mg/ml using 50 to 500 ml of D5W.

Administer I.V. infusion with an infusion pump or other controlled-delivery device.

Don’t exceed 500 mg in 30 minutes by I.V. infusion or 50 mg/min by I.V. injection because heart block or cardiac arrest may occur.

Anticipate that patient has reached maximum clinical response when ventricular tachycardia resolves, hypotension develops, or QRS complex is 50% wider than original width.

Expect to give first oral dose 3 to 4 hours procainamide hydrochloride 862 after last I.V. dose.

PATIENT SAFTY

Instruct patient to swallow procainamide tablets whole, without breaking, crushing, or chewing them.

If patient has trouble swallowing, tell her to crush regular-release tablets or open capsules and mix contents with food or fluid.

Instruct patient to take drug 1 hour before or 2 hours after meals with a full glass of water. Inform her that she may take drug with food if GI irritation develops.

Urge patient to obtain needed dental work before therapy starts or after blood count returns to normal because drug can cause myelosuppression and increased risk of bleeding and infection. Encourage good oral hygiene during therapy, and urge patient to consult prescriber before having dental procedures.

Advise patient to notify prescriber immediately about bruising, chills, diarrhea, fever, or rash.

Category

Chemical class: Phenothiazine, piperazine
Therapeutic class: Antianxiety, antiemetic, antipsychotic

Pregnancy category: Not rated

Indications

To control nausea and vomiting related to surgery

IV

OR INJECTION (PROCHLORPERAZINE EDISYLATE) Adults and adolescents. 5 to 10 mg at a rate not to exceed 5 mg/ml 15 to 30 min before anesthesia or during or after surgery, as needed. Dosage repeated once, if necessary. Maximum: 10 mg/dose, 40 mg daily.
I.M.INJECTION(PROCHLORPERAZINE EDISYLATE) Adults and adolescents. 5 to 10 mg 1 to 2 hr before anesthesia or during or after surgery, as needed. Repeated once in 30 min, if needed. Maximum: 10 mg/dose, 40 mg daily. To control severe nausea and vomiting (PROCHLORPERAZINE MALEATE) Adults and adolescents. 15 to 30 mg daily in the morning, or 10 mg every 12 hr. Maximum: 40 mg daily.

ORALL

(PROCHLORPERAZINE EDISYLATE) Adults and adolescents. 5 to 10 mg t.i.d. or q.i.d. Maximum: 40 mg daily. Children weighing 18 to 39 kg (40 to 86 lb).2.5 mg t.i.d. or 5 mg b.i.d. Maximum: 15 mg daily. Children weighing 14 to 18 kg (31 to 40 lb).2.5 mg b.i.d. or t.i.d. Maximum: 10 mg daily. Children weighing 9 to 14 kg (20 to 31 lb). 2.5 mg once or twice daily. Maximum: 7.5 mg daily. (PROCHLORPERAZINE MALEATE) Adults and adolescents. 5 to 10 mg t.i.d. or q.i.d. Maximum: 40 mg daily.

IV

OR INJECTION (PROCHLORPERAZINE EDISYLATE) Adults and adolescents. 2.5 to 10 mg at a rate not to exceed 5 mg/min. Maximum: 40 mg daily.
I.M.INJECTION(PROCHLORPERAZINE EDISYLATE) Adults and adolescents. 5 to 10 mg every 3 to 4 hr, p.r.n. Maximum: 40 mg daily. Children ages 2 to 12. 132 mcg/kg/dose to maximum of 10 mg on day 1; then increased as needed. Maximum: On day 1, 10 mg; thereafter, 25 mg daily for children ages 6 to 12, 20 mg daily for children ages 2 to 6. SUPPOSITORIES(PROCHLORPERAZINE) Adults and adolescents. 25 mg b.i.d. Children weighing 18 to 39 kg. 2.5 mg t.i.d. or 5 mg b.i.d. Maximum: 15 mg daily. Children weighing 14 to 18 kg. 2.5 mg b.i.d. or t.i.d. Maximum: 10 mg daily. Children weighing 9 to 14 kg. 2.5 mg once or twice daily. Maximum: 7.5 mg daily. To manage psychotic disorders, such as schizophrenia

ORALL

(PROCHLORPERAZINE EDISYLATE) prochlorperazine 863 P Adults and adolescents. 5 to 10 mg t.i.d. or q.i.d., increased gradually every 2 to 3 days, as needed and tolerated. Maximum: 150 mg daily. Children ages 2 to 12. 2.5 mg b.i.d. or t.i.d. Maximum: On day 1, 10 mg for all children; thereafter, 25 mg daily for children ages 6 to 12, 20 mg daily for children ages 2 to 6. (PROCHLORPERAZINE MALEATE) Adults and adolescents. 5 to 10 mg t.i.d. or q.i.d., increased gradually every 2 to 3 days, as needed and tolerated. Maximum: 150 mg daily.
I.M.INJECTION(PROCHLORPERAZINE EDISYLATE) Adults and adolescents. Initial: 10 to 20 mg, repeated every 2 to 4 hr, as prescribed, to bring symptoms under control (usually 3 to 4 doses). Maintenance: 10 to 20 mg every 4 to 6 hr. Maximum: 200 mg daily. Children ages 2 to 12. 132 mcg/kg/dose on day 1; then increased as needed. Maximum: On day 1, 10 mg for all children; thereafter, 25 mg daily for children ages 6 to 12, 20 mg/day for children ages 2 to 6. To treat anxiety short-term (PROCHLORPERAZINE MALEATE) Adults and adolescents. 15 mg daily in the morning, or 10 mg every 12 hr. Maximum: 20 mg/day for no longer than 12 wk.

ORALL

, (PROCHLORPERAZINE EDISYLATE) Adults and adolescents. 5 mg t.i.d. or q.i.d. Maximum: 20 mg daily for no longer than 12 wk.

IV

OR INJECTION (PROCHLORPERAZINE EDISYLATE) Adults and adolescents. 2.5 to 10 mg at no more than 5 mg/min. Maximum: 40 mg daily.
I.M.INJECTION(PROCHLORPERAZINE EDISYLATE) Adults and adolescents. 5 to 10 mg every 3 to 4 hr, p.r.n.
DOSAGE ADJUSTMENT Initial dose usually reduced and subsequent dosage increased more gradually for elderly, emaciated, and debilitated patients.

Mechanism of Action

Alleviates psychotic symptoms by blocking dopamine receptors, depressing release of selected hormones, and producing alphaadrenergic blocking effect in the brain. Prochlorperazine also alleviates nausea and vomiting by centrally blocking dopamine receptors in the medullary chemoreceptor trigger zone and by peripherally blocking the vagus nerve in the GI tract. Anticholinergic effects and alphaadrenergic blockade reduce anxiety by decreasing arousal and filtering internal stimuli to the brain stem reticular activating system. Route Onset Peak Duration P.O.,I.V., Up to several Up to Unknown I.M.,P.R. wk* 6 mo

Incompatibilities

Don’t mix prochlorperazine in same syringe with other . Precipitate may form when prochlorperazine edisylate is mixed in same syringe with morphine sulfate.

Contraindications

Age less than 2 years, blood dyscrasias, bone marrow depression, cerebral arteriosclerosis, coma, coronary artery disease, hepatic dysfunction, hypersensitivity to phenothiazines, myeloproliferative disorders, pediatric surgery, severe CNS depression, severe hypertension or hypotension, subcortical brain damage, use of large quantities of CNS depressants, weight less than 9 kg (20 lb)

Interactions

aluminumor magnesium-containing antacids, antidiarrheals (adsorbent): Possibly inhibited absorption of oral prochlorperazine amantadine, anticholinergics, antidyskinetics, antihistamines: Possibly intensified anticholinergic adverse effects, increased risk of prochlorperazine-induced hyperpyretic effect amphetamines: Decreased stimulant effect of amphetamines, decreased antipsychotic effect of prochlorperazine anticonvulsants: Lowered seizure threshold antithyroid : Increased risk of agranulocytosis apomorphine: Possibly decreased emetic response to apomorphine, additive CNS depression appetite suppressants: Possibly antagonized anorectic effect of appetite suppressants * For antipsychotic effects; unknown for other indications. (except for phenmetrazine) astemizole, cisapride, disopyramide, erythromycin, pimozide, probucol, procainamide: Additive QT interval prolongation, increased risk of ventricular tachycardia
beta blockers: Increased risk of additive hypotensive effects, irreversible retinopathy, arrhythmias, and tardive dyskinesia bromocriptine: Decreased effectiveness of bromocriptine
CNS depressants: Additive CNS depression dopamine: Possibly antagonized peripheral vasoconstriction (high doses of dopamine) ephedrine, epinephrine: Decreased vasopressor effects of these hepatotoxic : Increased risk of hepatotoxicity hypotension-producing : Possibly severe hypotension with syncope levodopa: Inhibited antidyskinetic effect of levodopa lithium: Reduced absorption of oral prochlorperazine, increased lithium excretion, increased extrapyramidal effects, possibly masking of early symptoms of lithium toxicity MAO inhibitors, maprotiline, tricyclic antidepressants: Possibly prolonged and intensified anticholinergic and sedative effects, increased antidepressant level, inhibited prochlorperazine metabolism, increased risk of neuroleptic malignant syndrome mephentermine: Possibly antagonized antipsychotic effect of prochlorperazine and vasopressor effect of mephentermine metrizamide: Increased risk of seizures opioid analgesics: Increased risk of CNS and respiratory depression, orthostatic hypotension, severe constipation, urine retention ototoxic : Possibly masking of some symptoms of ototoxicity, such as dizziness, tinnitus, and vertigo
phenytoin: Possibly inhibited phenytoin metabolism, increased risk of phenytoin toxicity thiazide diuretics: Possibly potentiated hyponatremia and water intoxication
alcohol use: Additive CNS depression

Side Efect

CNS: Akathisia, altered temperature regulation, dizziness, drowsiness, extrapyramidal reactions (such as dystonia, pseudoparkinsonism, tardive dyskinesia)
CV: Hypotension, orthostatic hypotension, tachycardia
EENT: Blurred vision, dry mouth, nasal congestion, ocular changes, pigmentary retinopathy
ENDO: Galactorrhea, gynecomastia
GI: Constipation, epigastric pain, nausea, vomiting
GU: Dysuria, ejaculation disorders, menstrual irregularities, urine retention
SKIN: Decreased sweating, photosensitivity, pruritus, rash
Other: Weight gain

Cautions

Prochlorperazine shouldn’t be used to treat dementia-related psychosis in the elderly because of increased mortality risk.

Avoid contact between skin and solution forms of prochlorperazine because contact dermatitis could result.

Inject I.M. form slowly, deep into upper outer quadrant of buttocks. Keep patient supine for 30 minutes after injection to minimize hypotensive effects.

Rotate I.M. injection sites to prevent irritation and sterile abscesses.

Be aware that I.V. form may be given undiluted as injection or diluted in isotonic solution as infusion (mesylate form requires dilution in at least 1 L). Both forms should be given at no more than 5 mg/minute.

Protect prochlorperazine from light.

Parenteral solution may develop slight yellowing that won’t affect potency. Don’t use if discoloration is pronounced or precipitate is present.

Expect antipsychotic effects to occur in 2 to 3 weeks, although range is days to months.
WARNING Monitor closely for numerous

Side Efect

that may be serious.

Adverse effects may occur up to 12 weeks after discontinuation of capsules.

PATIENT SAFTY

Instruct patient to take prochlorperazine with food or a full glass of milk or water to minimize GI distress.

Advise patient to swallow capsules whole, not to crush or chew them.

Instruct patient using suppository to refrigerate it for 30 minutes or hold it under running cold water before removing the wrapper if it softens during storage. prochlorperazine 865 P

Teach patient correct administration technique for suppository.

Caution patient on long-term therapy not to stop prochlorperazine abruptly; doing so may lead to such

Side Efect

as nausea, vomiting, and trembling.

Urge patient to avoid alcohol and OTC that may contain CNS depressants.

Advise patient to rise slowly from lying and sitting positions to minimize effects of orthostatic hypotension.

Urge patient to avoid hazardous activities because of the risk of drowsiness and impaired judgment and coordination.

Instruct patient to avoid excessive sun exposure and to wear sunscreen outdoors.

Urge patient to notify prescriber about involuntary movements and restlessness.

Explain that adverse effects may occur up to 12 weeks after stopping capsules.

Category

Chemical class: Progesterone derivative, steroid hormone
Therapeutic class: Antianorectic, anticachectic, antineoplastic, ovarian hormone replacement

Pregnancy category: D

(hydroxyprogesterone, megestrol [tablets], progesterone); X (levonorgestrel, medroxyprogesterone [parenteral], megestrol [parenteral and suspension], norethindrone, norgestrel); NR (medrogestone, medroxyprogesterone [tablets])

Indications

To treat renal cancer
I.M.INJECTION(MEDROXYPROGESTERONE) Adults and adolescents. Initial: 400 mg to 1 g every wk until improvement and stabilization. Maintenance: 400 mg or more every mo. To treat breast cancer (MEGESTROL) Adults and adolescents. 160 mg daily as single dose or in divided doses. To treat endometrial cancer (MEGESTROL) Adult and adolescent women.40 to 320 mg daily in divided doses.
I.M.INJECTION(MEDROXYPROGESTERONE) Adults and adolescents. Initial: 400 mg to 1 g every wk until improvement and stabilization. Maintenance: 400 mg or more every mo. To treat anorexia, cachexia, or significant weight loss in patients who have AIDS SUSPENSION (MEGESTROL) Adults and adolescents. 800 mg daily for the first mo, and then 400 or 800 mg daily for the next 3 mo. To treat endometriosis (NORETHINDRONE ACETATE) Adult and adolescent women.Initial: 5 mg daily for 2 wk, increased by 2.5 mg daily at 2-wk intervals to total dose of 15 mg daily. Maintenance: 15 mg daily for 6 to 9 mo unless temporarily discontinued because of breakthrough menstrual bleeding. As adjunct to treat endometrial shedding in menopausal women (MEDROGESTONE) Adult and adolescent women. 5 to 10 mg daily on days 15 through 25 of menstrual cycle. To treat secondary amenorrhea (MEDROGESTONE) Adult and adolescent women.5 to 10 mg daily on days 15 through 25 of menstrual cycle. (MEDROXYPROGESTERONE) Adult and adolescent women.5 to 10 mg daily for 5 to 10 days, starting anytime during menstrual cycle. (NORETHINDRONE ACETATE) Adult and adolescent women.2.5 to 10 mg daily on days 5 through 25 of menstrual cycle. Or, 2.5 to 10 mg daily for 5 to 10 days during last half of menstrual cycle. (PROGESTERONE) Adult and adolescent women.400 mg daily in evening for 10 days.
I.M.INJECTION(HYDROXYPROGESTERONE) Adult and adolescent women.375 mg as one-time dose.
I.M.INJECTION(PROGESTERONE) Adult and adolescent women.5 to 10 mg daily for 6 to 10 days. Or, 100 to 150 mg injected as single dose. VAGINAL GEL (PROGESTERONE) Adult and adolescent women.45 mg (1 applicatorful of 4% vaginal gel) every other day for up to 6 doses. Dosage increased, as needed, to 90 mg (1 applicatorful of 8% vaginal gel) every other day for up to 6 doses. To treat dysfunctional uterine bleeding (MEDROGESTONE) Adult and adolescent women.5 to 10 mg daily on days 15 through 25 of menstrual cycle. (MEDROXYPROGESTERONE) Adult and adolescent women.5 to 10 mg daily for 5 to 10 days, starting on day 16 or 21 of menstrual cycle. (NORETHINDRONE ACETATE) Adult and adolescent women.2.5 to 10 mg daily on days 5 through 25 of menstrual cycle. Or, 2.5 to 10 mg daily for 5 to 10 days during last half of menstrual cycle.
I.M.INJECTION(HYDROXYPROGESTERONE) Adult and adolescent women. 375 mg as one-time dose.
I.M.INJECTION(PROGESTERONE) Adult and adolescent women. 5 to 10 mg daily for 6 consecutive days. To induce menses (MEDROGESTONE) Adult and adolescent women.5 to 10 mg daily on days 15 through 25 of the menstrual cycle. (MEDROXYPROGESTERONE) Adult and adolescent women.10 mg daily for 10 days, starting on day 16 of menstrual cycle. Repeated for 2 or more cycles if bleeding is satisfactorily controlled.
I.M.INJECTION(HYDROXYPROGESTERONE) Adult and adolescent women. 125 to 250 mg on day 10 of menstrual cycle, repeated every 7 days until suppression is no longer desired. To prevent pregnancy (postcoital) (LEVONORGESTREL) Adult and adolescent women.0.75 mg as soon as possible within 72 hr of intercourse. Second dose given 12 hr later. To prevent pregnancy (NORETHINDRONE) Adult and adolescent women.0.35 mg daily, starting on day 1 of menstrual cycle and continuing uninterrupted through the year, whether or not menstrual bleeding occurs. (NORGESTREL) Adult and adolescent women. 0.075 mg daily starting on day 1 of menstrual cycle and continuing uninterrupted throughout the year, whether or not menstrual bleeding occurs.
I.M.INJECTION(MEDROXYPROGESTERONE) Adult and adolescent women. 150 mg every 3 mo. SUBDERMAL IMPLANT (LEVONORGESTREL) Adult and adolescent women. One set of implants surgically inserted every 2 yr.

Mechanism of Action

Progestins may diminish response to endogenous hormones in tumor cells by decreasing the number of steroid hormone receptors, causing a direct cytotoxic or antiproliferative effect on cell cycle growth and increased terminal cell differentiation. At higher doses, some progestins decrease adrenal production of estradiol and androstenedione, which may decrease estrogenor testosterone-sensitive tumors. Megestrol stimulates appetite and metabolic effects, which promotes weight gain. Progestins also bind to cytostolic receptors that are loosely bound in cell nucleus, increasing protein synthesis and improving cachexia. Progestins affect other hormones, especially estrogen, by reducing availability or stability of hormone receptor complex, progestins 867 P shutting off estrogen-responsive genes, or causing negative feedback mechanism that decreases number of functioning estrogen receptors. These actions allow menstrual cycle to function normally, alleviating amenorrhea and dysfunctional uterine bleeding and inducing menses. Progestins also act to transform proliferative uterine endometrium into a more differentiated, secretory one, which is the basis for using medroxyprogesterone to treat some types of amenorrhea. In a normal ovulatory cycle not resulting in pregnancy, decline in progesterone secretion caused by degeneration of corpus luteum in late luteal phase results in endometrial sloughing. A similar sloughing occurs after 5 to 10 days of medroxyprogesterone, provided that adequate estrogen-stimulated proliferation has occurred during follicular phase. Selected progestins also inhibit secretion of gonadotropins from pituitary gland, which prevents ovulation, follicular maturation, thickening of cervical mucus to prevent sperm penetration, and creation of an atrophic endometrium, resulting in contraceptive effect.

Contraindications

Active thromboembolic disorder; thrombophlebitis; significant hepatic disease; hypersensitivity to peanuts (progesterone), progestins, or their components; known or suspected breast cancer; pregnancy; undiagnosed genital, uterine, or urinary tract bleeding

Interactions

aminoglutethimide: Possibly decreased blood level of medroxyprogesterone carbamazepine, phenobarbital, phenytoin, rifabutin,
rifampin: Possibly decreased effectiveness of progestin thyroid hormone: Decreased thyroid hormone effectiveness

Side Efect

CNS: Altered or reduced coordination or speech, depression, dizziness, drowsiness, fatigue, headache, irritability, migraine, mood changes, nervousness, postmenopausal dementia, syncope, unusual tiredness or weakness
CV: Fluid retention; hypotension; numbness or pain in chest, arm, or leg; thromboembolism
ENDO: Adrenal insufficiency or suppression, breast pain or tenderness, Cushing’s syndrome, decreased T3resin uptake, delayed return of fertility in women, elevated thyroid-binding globulin, galactorrhea, hyperglycemia, vaginal spotting
EENT: Gingival bleeding, swelling, or tenderness; vision changes or loss
GI: Abdominal cramps or pain, diarrhea, nausea, vomiting
GU: Amenorrhea, breakthrough bleeding or metromenorrhagia, decreased libido, hypermenorrhea, ovarian enlargement or cysts
HEME: Clotting and bleeding abnormalities
MS: Back pain, decreased bone density, osteoporosis, osteoporotic fractures
RESP: Dyspnea
SKIN: Acne, alopecia, melasma, rash
Other: Anaphylaxis; facial fullness; hot flashes; injection or implantation site irritation, pain, or redness; weight gain

Cautions

Be aware that progestin/estrogen therapy shouldn’t be used to prevent cardiovascular disease or dementia.

Use progestins cautiously in patients with risk factors for arterial vascular disease, such as hypertension, diabetes mellitus, tobacco use, hypercholesterolemia, obesity, systemic lupus erythematosus, or a family or personal history of venous thromboembolism. Drug worsen these conditions.

Use progestins cautiously in patients who have CNS disorders, such as seizures or depression, because progestins may worsen these conditions.

Be aware that drug causes significant loss of bone mineral density in adolescence and early adulthood and isn’t recommended for long-term contraception. If other contraceptive methods are inadequate, evaluate bone mineral density routinely, as ordered.

Confirm that patient isn’t pregnant before giving progestin as a contraceptive.

Shake container vigorously for at least 1 minute before giving medroxyprogesterone acetate injection suspension or megestrol acetate oral suspension.

Inject parenteral medroxyprogesterone slowy, over 5 to 7 seconds, into deltoid muscle. Don’t inject into gluteal muscle to lessen absorption problems that may occur when patient sits on injection site. Pat site lightly after injection; don’t rub it.

Be aware that cyclical use of progestins is based on a menstrual cycle of 28 days.
WARNING Notify prescriber immediately if patient develops sudden vision loss, abnormal protrusion of eyeball, diplopia, papilledema, migraine, or other signs of thrombotic events. Expect to discontinue progestin if such signs occur.

Monitor patient for adrenal suppression, especially with megestrol therapy. If suspected, notify prescriber.

Expect to stop progestin/estrogen therapy in any woman who develops evidence of cancer; cardiovascular disease such as CVA, MI, pulmonary embolism, or venous thrombosis; or dementia.

PATIENT SAFTY

Explain risks of progestin/estrogen therapy, including breast, endometrial, or ovarian cancer; cardiovascular disease; dementia; and gallbladder disease, especially in postmenopausal women.

Instruct woman to notify prescriber if uterine bleeding continues longer than 3 months or if menstruation is delayed by 45 days.

Warn patient taking progestin for noncontraceptive purposes to use a contraceptive method to prevent pregnancy because drug may harm fetus.

Advise female patient to contact prescriber immediately if she suspects pregnancy or misses a menstrual period.

Stress importance of using a second method of birth control when taking other that could reduce contraceptive effectiveness of progestins.

Advise patient that some products may contain peanut oil. If she is allergic to peanuts, tell her to contact pharmacist to find out if prescribed progestin product contains peanut oil.

Advise female patient who vomits shortly after taking progestin-only oral contraceptive pill not to take another dose immediately thereafter but to wait until next scheduled dose before resuming therapy and to use an additional contraceptive method for 48 hours afterward.

Caution female patient who vomits within 1 hour of taking progestin for emergency contraception to contact prescriber about whether to repeat dose.

Teach woman how to use vaginal gel, if prescribed. Tell her to avoid using other vaginal products for 6 hours before and after to ensure gel’s complete absorption.

Direct patient to alert all prescribers about progestin therapy because certain blood tests may be affected.

Stress importance of good dental hygiene and regular dental checkups because elevated progestin level increases growth of normal oral flora, which may lead to gum tenderness, bleeding, or swelling.

Caution postmenopausal women about increased risk of dementia associated with progestin therapy.

Category

Chemical class: Phenothiazine derivative
Therapeutic class: Antiemetic, antihistamine, antivertigo, sedative-hypnotic

Pregnancy category: C

Indications

To prevent or treat motion sickness SYRUP, Adults and adolescents. 25 mg 30 to 60 min before travel and repeated 8 to 12 hr later, if needed. Maximum: 150 mg daily. To treat vertigo SYRUP, Adults and adolescents. 25 mg b.i.d., p.r.n. Maximum: 150 mg daily. Children age 2 and over. 0.5 mg/kg or 10 to 25 mg every 12 hr, p.r.n. SUPPOSITORIES Adults and adolescents. 25 mg b.i.d., p.r.n. Maximum: 150 mg daily. Children age 2 and over.0.5 mg/kg or 12.5 to 25 mg every 12 hr. To prevent or treat nausea and vomiting in certain types of anesthesia and surgery SYRUP, Adults and adolescents. Initial: 25 mg; then 10 to 25 mg every 4 to 6 hr, p.r.n. Maximum: 150 mg daily. Children age 2 and over. 0.25 to 0.5 mg/kg or 10 to 25 mg every 4 to 6 hr, p.r.n. I.V. OR

IM

Adults and adolescents. 12.5 to 25 mg every 4 hr, p.r.n. Maximum: 150 mg daily.
I.M.INJECTION Children age 2 and over. 0.25 to 0.5 mg/kg or 12.5 to 25 mg every 4 to 6 hr, p.r.n. SUPPOSITORIES Adults and adolescents. Initial: 25 mg; then 12.5 to 25 mg every 4 to 6 hr, p.r.n. Maximum: 150 mg daily. Children age 2 and over. 0.25 to 0.5 mg/kg or 12.5 to 25 mg every 4 to 6 hr. To treat signs and symptoms of allergic response SYRUP, Adults and adolescents. 10 to 12.5 mg q.i.d. before meals and at bedtime, p.r.n. Or, 25 mg at bedtime, p.r.n. Maximum: 150 mg daily. Children age 2 and over.0.125 mg/kg every 4 to 6 hr or 5 to 12.5 mg t.i.d., p.r.n. Or, 0.5 mg/kg or 25 mg at bedtime, p.r.n. I.V. INJECTION Adults and adolescents. 25 mg, repeated within 2 hr, if needed.
I.M.INJECTION, SUPPOSITORIES Adults and adolescents. 25 mg, repeated in 2 hr, p.r.n. Maximum: 150 mg daily. Children age 2 and over. 0.125 mg/kg every 4 to 6 hr or 6.25 to 12.5 mg t.i.d., p.r.n. Or, 0.5 mg/kg or 25 mg at bedtime, p.r.n. To provide nighttime, preoperative, or postoperative sedation SYRUP, Adults and adolescents. 25 to 50 mg as a single dose. Maximum: 150 mg daily. Children age 2 and over. 0.5 to 1 mg/kg or 10 to 25 mg as a single dose. Or, for preoperative sedation, 1.1 mg/kg along with 1.1 mg/kg of meperidine and appropriate dose of an atropine-like drug. I.V. INJECTION Adults and adolescents. 25 to 50 mg as a single dose. Or, for preoperative and postoperative sedation, 25 to 50 mg combined with appropriately reduced dosages of analgesics and anticholinergics.
I.M.INJECTION, SUPPOSITORIES Adults and adolescents. 25 to 50 mg as a single dose. Or, for preoperative and postoperative sedation, 25 to 50 mg combined with appropriately reduced dosages of analgesics and anticholinergics. Children age 2 and over.0.5 to 1 mg/kg or 12.5 to 25 mg as a single dose. Or, for preoperative sedation, 1.1 mg/kg along with 1.1 mg/kg of meperidine and an appropriate dose of an atropine-like drug. To relieve apprehension and promote sleep the night before surgery SYRUP, , SUPPOSITORIES Adults and adolescents. 50 mg along with 50 mg of meperidine and an appropriate dose of an atropine-like drug at bedtime on the night before surgery.
DOSAGE ADJUSTMENT Dosage usually decreased for elderly patients. To provide obstetric sedation I.V. OR

IM

Adults and adolescents. 50 mg for early stages of labor, followed by 1 or 2 doses of 25 to 75 mg after labor is established, repeated every 4 hr during normal labor. Route Onset Peak Duration P.O. 15–60 Unknown 4–6 hr min I.V. 3–5 min Unknown 4–6 hr I.M., P.R. 20 min Unknown 4–6 hr

Mechanism of Action

Competes with histamine for H1-receptor sites, thereby antagonizing many histamine effects and reducing allergy signs and symptoms. Promethazine also prevents motion sickness, nausea, and vertigo by acting centrally on medullary chemoreceptive trigger zone and by decreasing vestibular stimulation and labyrinthine function in the inner ear. It also promotes sedation and relieves anxiety by blocking receptor sites in CNS, directly reducing stimuli to the brain.

Contraindications

Angle-closure glaucoma; benign prostatic hyperplasia; bladder neck obstruction; bone marrow depression; breast-feeding; children under age 2; coma; hypersensitivity or history of idiosyncratic reaction to promethazine, other phenothiazines, or their components; hypertensive crisis; lower respiratory tract disorders (including asthma) promethazine hydrochloride 870 when used as an antihistamine; pyloroduodenal obstruction; stenosing peptic ulcer; use of large quantities of CNS depressants

Interactions

amphetamines: Decreased stimulant effect of amphetamines anticholinergics: Possibly intensified anticholinergic adverse effects anticonvulsants: Lowered seizure threshold appetite suppressants: Possibly antagonized anorectic effect of appetite suppressants
beta blockers: Increased risk of additive hypotensive effects, irreversible retinopathy, arrhythmias, and tardive dyskinesia bromocriptine: Decreased effectiveness of bromocriptine
CNS depressants: Additive CNS depression dopamine: Possibly antagonized peripheral vasoconstriction (high doses of dopamine) ephedrine, metaraminol, methoxamine: Decreased vasopressor response to these epinephrine: Blocked alpha-adrenergic effects of epinephrine, increased risk of hypotension guanadrel, guanethidine: Decreased antihypertensive effects of these hepatotoxic : Increased risk of hepatotoxicity hypotension-producing : Possibly severe hypotension with syncope levodopa: Inhibited antidyskinetic effects of levodopa
MAO inhibitors: Possibly prolonged and intensified anticholinergic and CNS depressant effects of promethazine metrizamide: Increased risk of seizures ototoxic : Possibly masking of some symptoms of ototoxicity, such as dizziness, tinnitus, and vertigo
quinidine: Additive cardiac effects
riboflavin: Increased riboflavin requirement
alcohol use: Additive CNS depression

Side Efect

CNS: Akathisia, CNS stimulation, confusion, dizziness, drowsiness, dystonia, euphoria, excitation, fatigue, hallucinations, hysteria, incoordination, insomnia, irritability, nervousness, neuroleptic malignant syndrome, paradoxical stimulation, pseudoparkinsonism, restlessness, sedation, seizures, syncope, tardive dyskinesia, tremor
CV: Bradycardia, hypertension, hypotension, tachycardia
EENT: Blurred vision; diplopia; dry mouth, nose, and throat; nasal congestion; tinnitus; vision changes
ENDO: Hyperglycemia
GI: Anorexia, cholestatic jaundice, ileus, nausea, rectal burning or stinging (suppository form), vomiting
GU: Dysuria
HEME: Agranulocytosis, leukopenia, thrombocytopenia, thrombocytopenic purpura
RESP: Apnea, respiratory depression, tenacious bronchial secretions
SKIN: Dermatitis, diaphoresis, jaundice, photosensitivity, rash, urticaria
Other: Angioedema, paradoxical reactions

Cautions

Use promethazine cautiously in children and elderly patients because they may be more sensitive to its effects, patients with cardiovascular disease or hepatic dysfunction because of potential adverse effects, patients with asthma because of anticholinergic effects, and patients with seizure disorders or those who take that may affect seizure threshold because drug may lower seizure threshold.

Inject I.M. form deep into large muscle mass, and rotate sites.
WARNING Avoid inadvertent intra-arterial injection of promethazine because it can cause arteriospasm. Also avoid injecting drug under skin; severe tissue damage and gangrene may develop from impaired circulation.

Give I.V. injection at no more than 25 mg/ min; rapid I.V. administration may produce a transient drop in blood pressure.
WARNING Monitor respiratory function because drug may suppress cough reflex and cause thickening of bronchial secretions, aggravating such conditions as asthma and COPD. Rarely, it may depress respirations and induce apnea.

Monitor patient’s hematologic status as ordered because promethazine may cause bone marrow depression, especially when used with other known marrow-toxic agents. Assess patient for signs and symptoms of infection or bleeding.
WARNING Monitor patient for evidence of promethazine hydrochloride 871 P neuroleptic malignant syndrome, such as fever, hypertension or hypotension, involuntary motor activity, mental changes, muscle rigidity, tachycardia, and tachypnea. Be prepared to provide supportive treatment and drug therapy, as prescribed.

Be aware that patient shouldn’t have intradermal allergen tests within 72 hours of receiving promethazine because drug may significantly alter flare response.

PATIENT SAFTY

Tell patient to use a calibrated device to ensure accurate doses of promethazine syrup.

Teach patient correct administration technique for suppository, if needed.

Advise patient to avoid OTC unless approved by prescriber.

Instruct patient to notify prescriber immediately if she has involuntary movements and restlessness.

Urge patient to avoid alcohol and other CNS depressants during therapy.

Instruct patient to avoid hazardous activities until drug’s CNS effects are known.

Suggest rinsing and use of sugarless gum or hard candy to relieve dry mouth.

Urge patient to avoid excessive sun exposure and to use sunscreen when outdoors.

Category

Chemical class: 3-Phenylpropriophenone
Therapeutic class: Class IC antiarrhythmic

Pregnancy category: C

Indications

To treat life-threatening ventricular arrhythmias
Adults. Initial: 150 mg every 8 hr; after 3 or 4 days, increased to 225 mg every 8 hr (U.S.) or 300 mg every 12 hr (Canada), if needed; after an additional 3 or 4 days, further increased to 300 mg every 8 hr, if needed. Maximum: 900 mg daily.

Mechanism of Action

Prolongs recovery period after myocardial repolarization by inhibiting sodium influx through myocardial cell membranes. This action prolongs the refractory period, causing myocardial automaticity, excitability, and conduction velocity to decline.

Contraindications

Bronchospastic disorders, such as asthma; cardiogenic shock; electrolyte imbalances; heart failure (uncontrolled); hypersensitivity to propafenone or its components; severe hypotension; sinus bradycardia or AV conduction disturbances (without artificial pacemaker)

Interactions

amiodarone: Possibly altered cardiac conduction and repolarization; possibly increased blood propafenone level anesthetics (local): Increased risk of adverse CNS effects antiarrhythmics, fluoxetine: Increased propafenone level and adverse CV effects cimetidine, erythromycin, ketoconazole, paroxetine, ritonavir, saquinavir, sertraline: Possibly increased blood propafenone level desipramine: Possibly increased blood level of desipramine or propafenone digoxin: Increased risk of digitalis toxicity haloperidol, imipramine, venlafaxine: Possibly increased levels of these metoprolol, propranolol: Increased blood level and half-life of these orlistat: Possibly decreased absorption of propafenone
quinidine: Decreased propafenone metabolism
rifampin: Possibly decreased propafenone level
warfarin: Increased blood warfarin level and risk of bleeding grapefruit juice: Possibly increased blood propafenone level

Side Efect

CNS: Dizziness, fatigue, headache
CV: Angina, AV block, bradycardia, heart failure, irregular heartbeat, tachycardia, ventricular arrhythmias
EENT: Altered taste, blurred vision, dry mouth
GI: Constipation, diarrhea, nausea, vomiting
SKIN: Rash propafenone hydrochloride 872

Cautions

Assess patient for electrolyte imbalances, such as hyperkalemia, before starting propafenone or any antiarrhythmic to reduce risk of adverse cardiac reactions.

Use propafenone cautiously in patients with heart failure or myocardial dysfunction because beta-blocking activity may further depress myocardial contractility.

Monitor ECG tracings, blood pressure, and pulse rate, particularly at start of therapy and with dosage increases.

PATIENT SAFTY

Instruct patient to take a missed dose if she remembers within 4 hours; otherwise, tell her to skip missed dose and to resume the regular dosing schedule.

Advise patient not to stop propafenone or change dosage without asking prescriber.

Urge patient to carry medical identification showing she that takes propafenone.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Urge patient to increase fluid intake and dietary fiber if she becomes constipated.

Explain that drug may cause an unusual taste. Advise patient to notify prescriber if taste interferes with compliance.

Category

Chemical class: Quaternary amine
Therapeutic class: Anticholinergic

Pregnancy category: C

Indications

As adjunct to treat peptic ulcer disease
Adults. 15 mg t.i.d. before meals and 30 mg at bedtime, adjusted as needed and tolerated. Maximum: 120 mg daily. Children. 0.375 mg/kg q.i.d., adjusted as needed and tolerated.
DOSAGE ADJUSTMENT For elderly patients with mild symptoms or patients of belowaverage weight, dosage possibly reduced to 7.5 mg t.i.d. or q.i.d.

Mechanism of Action

Prevents the neurotransmitter acetylcholine from combining with receptors on postganglionic parasympathetic nerve terminal, thereby reducing smooth-muscle spasms in the GI system, slowing GI motility, and inhibiting gastric acid secretion. All these effects help to heal peptic ulcers. Route Onset Peak Duration P.O. Unknown Unknown 6 hr

Contraindications

Adhesions between iris and lens, angleclosure glaucoma, hemorrhage accompanied by hemodynamic instability, hepatic dysfunction, hypersensitivity to propantheline or its components, ileus, myasthenia gravis, myocardial ischemia, obstructive GI or urinary disease, renal dysfunction, severe ulcerative colitis, tachycardia

Interactions

amantadine, other anticholinergics, tricyclic antidepressants: Additive anticholinergic effects antacids, antidiarrheals (adsorbent): Possibly reduced absorption of propantheline antimyasthenics: Possibly further reduction in intestinal motility atenolol: Increased effects of atenolol cyclopropane: Possibly ventricular arrhythmias digoxin: Possibly digitalis toxicity
haloperidol: Decreased antipsychotic effect of haloperidol in schizophrenic patients
ketoconazole: Decreased ketoconazole absorption metoclopramide: Possibly decreased metoclopramide effect on GI motility opioid analgesics: Increased risk of severe constipation and urine retention phenothiazines: Possibly decreased antipsychotic effects potassium chloride: Possibly increased severity of potassium chloride–induced GI ulceration, stricture, or perforation urinary alkalizers: Delayed urinary excretion of propantheline

Side Efect

CNS: Dizziness, excitement, insomnia, nervousness, paradoxical CNS stimulation
CV: Palpitations, tachycardia
EENT: Blurred vision; dry mouth, nose, and throat
GI: Constipation, dysphagia, heartburn, ileus, nausea, vomiting
GU: Impotence, urinary hesitancy, urine retention
SKIN: Decreased sweating, dry skin, flushing

Cautions

Don’t administer propantheline within 1 hour of antacids or antidiarrheals.

Monitor elderly patients closely; they may respond to usual dose with agitation, confusion, drowsiness, or excitement.
WARNING Drug can interfere with sweating reflex, increasing the risk of heatstroke.

PATIENT SAFTY

Instruct patient to take propantheline 30 to 60 minutes before meals and at bedtime, as prescribed.

Inform patient that drug may cause dizziness. Urge her to avoid hazardous activities until drug’s CNS effects are known.

Encourage patient to increase fluid and fiber intake to decrease constipation. Instruct her to report persistent constipation and urine retention.

Advise patient to avoid excessive exposure to heat to reduce risk of heat prostration and heatstroke.

Suggest that patient relieve dry mouth with frequent rinsing and sugar-free hard candy or gum.

Category

Chemical class: 2,6-diisopropylphenol derivative
Therapeutic class: Sedative-hypnotic

Pregnancy category: B

Indications

To provide sedation for critically ill patients in intensive care

IV

Adults. 2.8 to 130 mcg/kg/min. Usual: 27 mcg/kg/min.
DOSAGE ADJUSTMENT For elderly, debilitated, or American Society of Anesthesiologists Physical Status (ASA-PS) III or IV patients, induction dose decreased and maintenance rate slower.

Mechanism of Action

Decreases cerebral blood flow, cerebral metabolic oxygen consumption, and intracranial pressure and increases cerebrovascular resistance, which may play a role in propofol’s hypnotic effects. Route Onset Peak Duration I.V. Within Unknown 3–5 min 40 sec

Incompatibilities

Don’t mix propofol with other before giving. Don’t give propofol through same I.V. line as blood or plasma products because globular component of emulsion will aggregate.

Contraindications

Hypersensitivity to propofol or its components, to eggs or egg products, or to soybeans or soy products

Interactions

CNS depressants: Additive CNS depressant, respiratory depressant, and hypotensive effects; possibly decreased emetic effects of opioids droperidol: Possibly decreased control of nausea and vomiting
alcohol use: Additive CNS depressant, respiratory depressant, and hypotensive effects

Side Efect

CV: Bradycardia, hypotension
GI: Nausea, vomiting
MS: Involuntary muscle movement (transient)
RESP: Apnea
Other: Anaphylaxis, injection site burning, pain, or stinging

Cautions

Use propofol cautiously in patients with cardiac disease, peripheral vascular disease, impaired cerebral circulation, or increased intracranial pressure because drug may aggravate these disorders.

To dilute before administration, use only D5W for final solution of 2 mg/ml or more.

Consult prescriber about pretreating injection site with 1 ml of 1% lidocaine to minimize pain, burning, or stinging that may occur. If ordered, lidocaine shouldn’t be added to propofol solution in quantities greater than 20 mg/200 mg propofol because emulsion may become unstable. Giving drug through a larger vein in forearm or antecubital fossa also may minimize injection site discomfort.

Shake container well before using, administer drug promptly after opening, and use vial for a single patient. Use prefilled syringes within 6 hours of opening.

Use a drop counter, syringe pump, or volumetric pump to safely control infusion rate. Don’t infuse drug through filter with a pore size of less than 5 microns; doing so could cause emulsion to break down.

Discard unused portion of propofol solution plus reservoirs, I.V. tubing, and solutions immediately after or within 12 hours of administration (6 hours if propofol was transferred from original container) to prevent bacterial growth in stagnant solution. Also, protect solution from light.

Dosage must be tapered before stopping therapy. Stopping abruptly will cause rapid awakening, anxiety, agitation and resistance to mechanical ventilation.

Expect patient to recover from sedation within 8 minutes.
WARNING Monitor patient for propofol infusion syndrome, especially with prolonged high-dose infusions. It may cause severe metabolic acidosis, hyperkalemia, lipemia, rhabdomyolysis, hepatomegaly and cardiac and renal failure. Alert prescriber at once and be prepared to provide emergency supportive care as ordered.

PATIENT SAFTY

Urge patient and family to voice concerns and ask questions before administration.

Reassure patient that she’ll be monitored closely during administration and that vital functions will be supported as needed.

Category

Chemical class: Synthetic opioid
Therapeutic class: Analgesic

Pregnancy category: Not rated

Controlled substance schedule: IV

Indications

To relieve mild to moderate pain , ORAL SUSPENSION, (PROPOXYPHENE NAPYSLATE)
Adults. 100 mg every 4 hr, p.r.n. Maximum: 600 mg daily. ,
Adults. 65 mg every 4 hr, p.r.n. Maximum: 390 mg daily. Route Onset Peak Duration P.O. 15–60 min 2 hr 4–6 hr

Mechanism of Action

Produces analgesia through a synergistic analgesic effect. Propoxyphene strongly agonizes mu receptors, blocking release of such inhibitory neurotransmitters as gamma-aminobutyric acid (GABA) and acetylcholine. It also mediates analgesia by changing pain perception at spinal cord and higher CNS levels and by altering emotional response to pain.

Contraindications

Hypersensitivity to propoxyphene or its components (including acetaminophen and aspirin), respiratory depression, severe asthma, upper airway obstruction, use within 14 days of MAO inhibitor therapy

Interactions

amphetamines: Possibly fatal seizures (with propoxyphene overdose) anticholinergics: Increased risk of severe constipation and urine retention antidiarrheals: Severe constipation, possibly increased CNS depression antihypertensives: Possibly exaggerated antihypertensive response buprenorphine: Possibly decreased propoxyphene effectiveness, increased respiratory depression carbamazepine: Possibly carbamazepine toxicity
CNS depressants: Increased CNS and respiratory depression, hypotensive effects, and propoxyphene 875 P risk of habituation hydroxyzine: Increased analgesic, CNS depressant, and hypotensive effects
MAO inhibitors: Severe, possibly fatal reactions, including hypertensive crisis metoclopramide: Possibly antagonized effects of metoclopramide on GI motility naloxone: Antagonized analgesic and CNS and respiratory depressant effects of propoxyphene
naltrexone: Risk of withdrawal symptoms in patients dependent on propoxyphene, possibly decreased analgesic effect neuromuscular blockers: Additive respiratory depressant effects opioid analgesics: Additive CNS and respiratory depressant and hypotensive effects
warfarin: Increased anticoagulation effects
alcohol use: Increased CNS and respiratory depression, hypotensive effects, and risk of habituation nicotine chewing gum, other smoking deterrents, smoking cessation: Decreased effectiveness of propoxyphene

Side Efect

CNS: Dizziness, drowsiness, fatigue, insomnia, light-headedness, malaise, nervousness, sedation, tremor
CV: Orthostatic hypotension, tachycardia
EENT: Blurred vision, diplopia, dry mouth, tinnitus
GI: Abdominal cramps, anorexia, constipation, nausea, vomiting
GU: Decreased urine output
MS: Muscle weakness
RESP: Dyspnea, respiratory depression, wheezing
SKIN: Facial flushing, pruritus, rash, urticaria
Other: Psychological dependence

Cautions

Be aware that propoxyphene shouldn’t be used in patients who are suicidal or prone to addiction because of risk of overdose.

Use drug cautiously in patients who take CNS depressants such as tranquilizers or antidepressants and patients who use alcohol in excess because of risk of overdose.

Use propoxyphene cautiously in patients with hepatic or renal dysfunction because delayed elimination may occur. Monitor hepatic and renal function test results.
WARNING Be aware that long-term, highdose propoxyphene therapy may lead to psychological dependence in some people. Assess for opioid and alcohol use, which increase risk of drug abuse or dependence.

Be aware drug is also available in combination products with aspirin or acetaminophen and caffeine.

Be aware that abruptly discontinuing drug can result in withdrawal symptoms.

PATIENT SAFTY

Inform patient that she may take propoxyphene with food if she has GI distress.

Caution patient not to take more than prescribed amount because drug may be addictive or cause accidental overdose.

Inform patient that drug may cause blurred vision, drowsiness, dizziness, and impaired judgment and coordination. Urge her to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to avoid alcohol and other sedatives while taking drug.

Advise smokers to inform prescriber if they try to stop smoking during propoxyphene therapy because increased dosage may be needed for effective analgesia.

Urge patient to notify prescriber immediately if pain isn’t relieved or worsens.

Category

Chemical class: Beta-adrenergic blocker
Therapeutic class: Antianginal, antiarrhythmic, antihypertensive, anti-MI, antimigraine, antitremor, hypertrophic cardiomyopathy and pheochromocytoma therapy adjunct

Pregnancy category: C

Indications

To manage hypertension
Adults. Initial: 80 mg daily, increased gradually up to 160 mg daily Maximum: 640 mg daily. XL (INNOPRAN XL)
Adults. Initial: 80 mg once daily at bedtime, increased, as needed, to 120 mg once daily at bedtime.

ORALL

,
Adults. Initial: 40 mg b.i.d., increased gradually to 120 to 240 mg daily, as needed. Maximum: 640 mg daily. Children. Initial: 0.5 to 1 mg/kg daily in divided doses b.i.d. to q.i.d., adjusted as needed. Maintenance: 2 to 4 mg/kg daily in divided doses b.i.d. To treat chronic angina
Adults. Initial: 80 mg daily, increased every 3 to 7 days, as prescribed. Maximum: 320 mg/day.

ORALL

,
Adults. 80 to 320 mg daily in divided doses b.i.d., t.i.d., or q.i.d. To treat supraventricular arrhythmias and ventricular tachycardia

ORALL

,
Adults. 10 to 30 mg t.i.d. or q.i.d., adjusted as needed. I.V. INJECTION
Adults. 1 to 3 mg at a rate not to exceed 1 mg/min; repeated after 2 min and again after 4 hr, if needed. Children. 0.01 to 0.1 mg/kg at a rate not to exceed 1 mg/min; repeated every 6 to 8 hr, as needed. Maximum: 1 mg/dose. To control tremor

ORALL

,
Adults. Initial: 40 mg b.i.d., adjusted as needed and prescribed. Maximum: 320 mg daily. To prevent vascular migraine headaches
Adults. Initial: 80 mg daily, increased gradually, as needed. Maximum: 240 mg daily.

ORALL

,
Adults. Initial: 20 mg q.i.d., increased gradually, as needed. Maximum: 240 mg daily. As adjunct to treat hypertrophic cardiomyopathy

ORALL

,
Adults. 20 to 40 mg t.i.d. or q.i.d., adjusted as needed. As adjunct to manage pheochromocytoma

ORALL

,
Adults. For operable tumors, 20 mg t.i.d. to 40 mg t.i.d. or q.i.d. for 3 days before surgery, concurrently with an alpha blocker. For inoperable tumors, 30 to 160 mg daily in divided doses. To prevent MI

ORALL

,
Adults. 180 to 240 mg daily in divided doses.
DOSAGE ADJUSTMENT Dosage increased or decreased for elderly patients, depending on sensitivity to propranolol. Route Onset Peak Duration P.O. Unknown 1–1.5 hr* Unknown

Mechanism of Action

Through beta-blocking action, propranolol:

prevents arterial dilation and inhibits renin secretion, resulting in decreased blood pressure (in hypertension and pheochromocytoma) and relief of migraine headaches

decreases heart rate, which helps resolve tachyarrhythmias

improves myocardial contractility, which helps ease symptoms of hypertrophic cardiomyopathy

decreases myocardial oxygen demand, which helps prevent anginal pain and death of myocardial tissue. In addition, peripheral beta-adrenergic blockade may play a role in propranolol’s ability to alleviate tremor.

Contraindications

Asthma, cardiogenic shock, greater than first-degree AV block, sick sinus syndrome, or sinus bradycardia (unless pacemaker in place); heart failure (unless secondary to tachyarrhythmia responsive to propranolol), hypersensitivity to propranolol or its components

Interactions

ACE inhibitors: Increased risk of hypotension, especially in presence of acute MI allergen immunotherapy, allergenic extracts for skin testing: Increased risk of serious systemic

Side Efect

or anaphylaxis amiodarone: Additive depressant effects on conduction, negative inotropic effects anesthetics (hydrocarbon inhalation): propranolol hydrochloride 877 P * For regular-release form; unknown for form. Increased risk of myocardial depression and hypotension
beta blockers: Additive beta blockade effects bupivacaine, lidocaine, mepivacaine: Decreased clearance of these , possibly increased risk of toxicity calcium channel blockers, clonidine, diazoxide, guanabenz, resperpine, other hypotension-producing : Additive hypotensive effect and, possibly, other beta blockade effects catecholamine-depleting , such as reserpine: Increased risk of hypotension, bradycardia, vertigo, syncope, and orthostatic hypotension
cimetidine: Possibly interference with propranolol clearance digitalis glycosides: Increased risk of bradycardia diltiazem: Increased risk of bradycardia, hypotension, high-degree heart block, and heart failure dobutamine, isoproterenol: Reversed effects of propranolol doxazosin, terazosin: Increased risk of orthostatic hypotension epinephrine: Increased risk of uncontrolled hypertension estrogens: Decreased antihypertensive effect of propranolol fentanyl, fentanyl derivatives: Possibly increased risk of initial bradycardia after induction doses of fentanyl or a derivative (with long-term propranolol use) glucagon: Possibly blunted hyperglycemic response insulin, oral antidiabetic : Possibly impaired glucose control, masking of tachycardia in response to hypoglycemia MAO inhibitors, tricyclic antidepressants: Increased risk of significant hypertension neuroleptic : Increased risk of hypotension and cardiac arrest neuromuscular blockers: Possibly potentiated and prolonged action of these
NSAIDs: Possibly decreased hypotensive effects phenothiazines: Increased blood levels of both
phenytoin: Additive cardiac depressant effects (with parenteral phenytoin) prazosin: Increased risk of first-dose hypotension propafenone: Increased blood level and halflife of propranolol
quinidine: Increased propranolol level, resulting in higher degrees of beta blockade and orthostatic hypotension sympathomimetics, xanthines: Possibly mutual inhibition of therapeutic effects thyroxine: Possibly decreased T3level verapamil: Increased risk of bradycardia, heart failure, and cardiovascular collapse
warfarin: Increased risk of bleeding alcohol: Possibly increased plasma propranolol level nicotine chewing gum, smoking cessation, smoking deterrents: Increased therapeutic effects of propranolol

Side Efect

CNS: Anxiety, depression, dizziness, drowsiness, fatigue, fever, insomnia, lethargy, nervousness, weakness
CV: AV conduction disorders, cold limbs, heart failure, hypotension, sinus bradycardia
EENT: Dry eyes, laryngospasm, nasal congestion, pharyngitis
GI: Abdominal pain, constipation, diarrhea, nausea, vomiting
GU: Impotence, peyronie’s disease, sexual dysfunction
HEME: Agranulocytosis
MS: Muscle weakness
RESP: Bronchospasm, dyspnea, respiratory distress, wheezing
SKIN: Alopecia, erythema multiforme, erythematous rash, exfoliative dermatitis, psoriasiform rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, flulike symptoms, systemic lupuslike reaction

Cautions

Use propranolol cautiously in patients with bronchospastic lung disease because it may induce asthmatic attack.

Monitor blood pressure, apical and radial pulses, fluid intake and output, daily weight, respiration, and circulation in extremities before and during therapy.

Give I.V. injection at no more than 1 mg/ minute.
WARNING Monitor ECG continuously, as ordered, when giving I.V. injection. Have emergency and equipment available in case of hypotension or cardiac arrest.

Protect injection solution from light. propranolol hydrochloride 878

Because drug’s negative inotropic effect can depress cardiac output, monitor cardiac output in patients with heart failure, particularly those with severely compromised left ventricular dysfunction.

Be aware that propranolol can mask tachycardia in hyperthyroidism and that abrupt withdrawal in patients with hyperthyroidism or thyrotoxicosis can cause thyroid storm.

Monitor diabetic patient taking an antidiabetic because propranolol can prolong hypoglycemia or promote hyperglycemia. It also can mask signs of hypoglycemia, especially tachycardia, palpitations, and tremor, but it doesn’t suppress diaphoresis or hypertensive response to hypoglycemia.
WARNING Be aware that stopping drug abruptly may cause myocardial ischemia, MI, ventricular arrhythmias, or severe hypertension, especially in patients with cardiac disease. It also may cause increased intraocular pressure to return. Dosage should be reduced gradually.

PATIENT SAFTY

Instruct patient to take propranolol at the same time every day.

Caution patient not to change dosage without consulting prescriber and not to stop taking drug abruptly.

Advise patient to notify prescriber immediately if she has shortness of breath.

Instruct diabetic patient to regularly check blood glucose level and urine for ketones.

Advise patient to consult prescriber before taking OTC , especially cold products.

Urge patient to avoid hazardous activities until CNS effects of drug are known.

Category

Chemical class: Thiourea derivative
Therapeutic class: Antithyroid

Pregnancy category: D

Indications

To treat hyperthyroidism Adults and adolescents. Initial: For mild to moderate hyperthyroidism, 300 to 900 mg daily in 1 to 4 divided doses until patient becomes euthyroid; for severe hyperthyroidism, 300 to 1,200 mg daily in 1 to 4 divided doses until patient becomes euthyroid. Maintenance: 50 to 600 mg daily in 1 to 4 divided doses. Children age 10 and over. Initial: 50 to 300 mg daily in 1 to 4 divided doses. Maintenance: Adjusted based on response to initial dosage. Children ages 6 to 10. Initial: 50 to 150 mg/ day in 1 to 4 divided doses. Maintenance: Adjusted based on response to initial dosage. Neonates. 10 mg/kg daily in divided doses. As adjunct to treat thyrotoxic crisis Adults and adolescents. 200 to 400 mg every 4 hr on day 1 plus other measures. Dosage gradually decreased as crisis subsides.
DOSAGE ADJUSTMENT If creatinine clearance is 10 to 50 ml/min/1.73 m2, recommended dosage reduced by 25%; if creatinine clearance is less than 10 ml/min/1.73 m2, recommended dosage reduced by 50%. Route Onset Peak Duration P.O. Unknown 17 wk Unknown

Mechanism of Action

Inhibits conversion of peripheral thyroxine to triiodothyronine by interfering with incorporation of iodide into thyroglobulin; drug remains iodinated and degraded in thyroid gland. Diversion of oxidized iodine away from thyroglobulin diminishes thyroid hormone synthesis and levels of circulating thyroid hormone.

Contraindications

Breast-feeding, hypersensitivity to propylthiouracil or its components

Interactions

amiodarone, iodinated glycerol, iodine, potaspropylthiouracil 879 P sium iodide: Decreased efficacy of propylthiouracil digoxin: Risk of digitalis toxicity oral anticoagulants: Possibly enhanced anticoagulant effect sodium iodide 131 (radioactive iodine,131I): Decreased thyroid uptake of131I

Side Efect

CNS: Dizziness, paresthesia, peripheral neuropathy
CV: Vasculitis
ENDO: Hypothyroidism
GI: Abdominal pain, hepatotoxicity, nausea, vomiting
HEME: Agranulocytosis, leukopenia
MS: Arthralgia, joint redness or swelling
SKIN: Pruritus, rash, urticaria
Other: Lupuslike symptoms

Cautions

Monitor CBC, PT, and liver and thyroid function test results in patients taking propylthiouracil. Elevated serum triiodothyronine (T3) level may be the sole indicator of inadequate treatment.

Expect to stop drug 3 to 4 days before 131I treatment to prevent decreased thyroid uptake of131I; therapy may be resumed 3 to 5 days after radiation, if needed.

Serum T3and thyroxine levels should decrease after about 3 weeks of therapy.

Expect to decrease beta blocker or theophylline dosage once patient is euthyroid.

Monitor liver function, especially during first 6 months of therapy, because drug may cause liver failure, need for liver transplant, or death. Expect to stop drug at first sign of liver dysfunction (fatigue, weakness, vague abdominal pain, loss of appetite, itching, easy bruising, jaundice).

PATIENT SAFTY

Instruct patient to take drug with meals to decrease risk of adverse GI reactions.

Urge patient to avoid dietary sources of iodine, such as iodized salt and shellfish.

Tell patient to check pulse rate and weight daily and to report increased heart rate and excessive weight loss to prescriber.

Urge patient to report signs and symptoms of infection, such as fever and sore throat, or signs and symptoms that could reflect hepatic dysfunction, such as anorexia and right-upper-quadrant pain.

Instruct patient to notify prescriber immediately if she becomes pregnant.

Advise patient to report signs and symptoms of hypothyroidism, such as cold intolerance, depression, and increased fatigue.

Tell patient to ask prescriber before using OTC cold (some contain iodides).

Advise patient to notify prescriber immediately if he has fatigue, weakness, vague abdominal pain, loss of appetite, itching, easy bruising, or yellowing of eyes or skin.

Category

Chemical class: Simple low-molecularweight protein
Therapeutic class: Heparin antagonist

Pregnancy category: C

Indications

To treat heparin toxicity or hemorrhage associated with heparin therapy I.V. INJECTION Adults and children. 1 mg for each 100 units of heparin to be neutralized, or as indicated by coagulation test results. Maximum: 100 mg (within 2-hr period). Route Onset Peak Duration I.V. 5 min Unknown 2 hr

Mechanism of Action

Neutralizes anticoagulant activity. A strong basic polypeptide, protamine combines with strongly acidic heparin complex to form an inactive stable salt, thereby neutralizing anticoagulant activity of both .

Incompatibilities

Don’t mix protamine sulfate in same syringe with other unless they’re known to be compatible. Several cephalosporins, penicillins, and other antibiotics are incompatible.

Contraindications

Allergy to fish, hypersensitivity to protamine or its components

Interactions

heparin: Neutralized anticoagulant effect of both

Side Efect

CNS: Weakness
CV: Bradycardia, hypertension, hypotension, shock
GI: Nausea, vomiting
HEME: Unusual bleeding or bruising
RESP: Dyspnea, pulmonary edema (noncardiogenic), pulmonary hypertension
SKIN: Flushing, sensation of warmth
Other: Anaphylaxis

Cautions

Expect to administer I.V. protamine undiluted. However, dilute drug if needed (for patients other than neonates) with 5 ml of bacteriostatic water for injection containing 0.9% benzyl alcohol. For neonates, reconstitute with preservative-free sterile water for injection.

Inject drug slowly at 5 mg/minute; administer no more than 50 mg in 10 minutes or 100 mg in 2 hours.
WARNING Be aware that rapid delivery may cause severe hypotension and anaphylaxis.

Be prepared to obtain coagulation studies (APTT, activated clotting time) 5 to 15 minutes after giving drug and to repeat them in 2 to 8 hours to detect heparinrebound hypotension, shock, and bleeding.

Monitor vital signs, hemodynamic parameters, and fluid intake and output, and assess for flushing sensation.

Have fluids—epinephrine 1:1,000, dobutamine, or dopamine—available for allergic or hypotensive reactions.

Be aware that men with vasectomy have an increased risk of hypersensitivity reaction because of possible accumulation of antiprotamine antibodies.

PATIENT SAFTY

Instruct patient to report

Side Efect

immediately.

Category

Chemical class: Dibenzocycloheptene derivative
Therapeutic class: Antidepressant

Pregnancy category: Not rated

Indications

To treat depression
Adults. Initial: 5 to 10 mg t.i.d. or q.i.d., increased every wk by 10 mg daily, as needed. Maximum: 60 mg daily. Children age 12 and over. Initial: 5 mg t.i.d., increased as needed.
DOSAGE ADJUSTMENT For elderly patients, initial dosage limited to 5 mg t.i.d., then adjusted as needed. Route Onset Peak Duration P.O. 2–3 wk Unknown Unknown

Mechanism of Action

May block reuptake of norepinephrine and serotonin (and possibly other neurotransmitters) at neuronal membranes, thus enhancing their effects at postsynaptic receptors. These neurotransmitters may play a role in relieving depression symptoms.

Contraindications

Acute recovery phase after MI, hypersensitivity to protriptyline or its components, use within 14 days of MAO inhibitor therapy

Interactions

amantadine, anticholinergics, antidyskinetics, antihistamines: Additive anticholinergic effects, potentiated effects of antihistamines or protriptyline, possibly impaired detoxification of atropine and related anticonvulsants: Possibly lowered seizure threshold and decreased anticonvulsant effectiveness; enhanced CNS depression antithyroid : Possibly agranulocytosis barbiturates, carbamazepine: Decreased therapeutic effects of protriptyline bupropion, clozapine, cyclobenzaprine, haloperidol, loxapine, maprotiline, molindone, phenothiazines,
thioxanthenes: Prolonged and intensified anticholinergic and sedative effects, lowered seizure threshold, increased risk of neuroleptic malignant syndrome; increased blood protriptyline level and inhibited phenothiazine metabolism (with phenothiazine use)
cimetidine: Increased risk of protriptyline toxicity clonidine, guanadrel, guanethidine: Decreased hypotensive effects; increased CNS depression (with clonidine use)
CNS depressants: Possibly serious potentiation of CNS and respiratory depression and hypotensive effect disulfiram, ethchlorvynol: Possibly transient delirium; increased CNS depression (with ethchlorvynol use) fluoxetine: Increased protriptyline level
MAO inhibitors: Increased risk of hyperpyretic crisis, severe seizures, and death
methylphenidate: Possibly antagonized effects of methylphenidate and increased blood protriptyline level metrizamide: Increased risk of seizures naphazoline, oxymetazoline, phenylephrine, xylometazoline: Possibly increased vasopressor effects of these oral anticoagulants: Possibly increased anticoagulant activity pimozide, probucol: Possibly prolonged QT interval and ventricular tachycardia sympathomimetics: Possibly potentiated cardiovascular effects, decreased vasopressor effects of ephedrine and mephentermine thyroid hormones: Increased therapeutic and toxic effects of both
alcohol use: Possibly increased response to alcohol

Side Efect

CNS: Agitation, ataxia, confusion, dizziness, drowsiness, exacerbation of psychosis, extrapyramidal reactions, fatigue, lack of coordination, paresthesia, peripheral neuropathy, suicidal ideation, tremor, weakness
CV: Arrhythmias, including heart block and tachycardia; hypertension; hypotension; MI; orthostatic hypotension; palpitations; stroke
EENT: Black tongue, blurred vision, dry mouth, increased intraocular pressure, lacrimation, stomatitis, tongue swelling
ENDO: Hyperglycemia, hypoglycemia
GI: Abdominal cramps, anorexia, constipation, diarrhea, epigastric discomfort, hepatic dysfunction, nausea, vomiting
GU: Impotence, libido changes, nocturia, urinary frequency and hesitancy, urine retention
SKIN: Diaphoresis, petechiae, photosensitivity, rash, urticaria
Other: Facial edema, weight gain or loss

Cautions

Use protriptyline cautiously in patients with a history of seizures because drug can lower seizure threshold.

Use cautiously in patients with a history of urine retention or increased intraocular pressure because of drug’s autonomic activity.
WARNING Avoid giving protriptyline with an MAO inhibitor. If patient is being switched from an MAO inhibitor to protriptyline, make sure MAO inhibitor has been discontinued for 14 days before starting protriptyline.

Watch patients closely (especially children, adolescents, and young adults) for suicidal tendencies, particularly when therapy starts or dosage changes, because depression may worsen temporarily during these times, possibly leading to suicidal ideation.

PATIENT SAFTY

Inform patient that protriptyline therapy may take several weeks to reach full effect.

Instruct patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to change position slowly to minimize orthostatic hypotension.

Urge patient to avoid alcohol while taking drug.

Suggest drinking water and using sugarless gum or hard candy to relieve dry mouth.

Advise patient to avoid sunlight and tanning booths and to wear protective clothing, a hat, and sunscreen when outdoors.

Instruct diabetic patient to check blood glucose level frequently during first few weeks of protriptyline therapy.

Urge family or caregiver to watch patient for suicidal tendencies, especially when therapy starts or dosage changes and particularly if patient is a child, teenager, or young adult.

Category

Chemical class: Pyrazine analogue of nicotinamide
Therapeutic class: Antitubercular

Pregnancy category: C

Indications

As adjunct to treat tuberculosis, along with other antitubercular Adults and children. 15 to 30 mg/kg daily; or, 50 to 70 mg/kg 2 or 3 times/wk. Maximum: For daily regimen, 2 g daily; for twice/wk regimen, 4 g daily; for 3-times/wk regimen, 3 g daily.
DOSAGE ADJUSTMENT For patients with HIV infection, 20 to 30 mg/kg daily for first 2 mo of therapy.

Mechanism of Action

Inhibits growth of Mycobacterium tuberculosis by decreasing pH level; exhibits bactericidal or bacteriostatic action, depending on blood pyrazinamide level.

Contraindications

Acute gout, hypersensitivity to pyrazinamide or its components, severe hepatic damage

Interactions

allopurinol, colchicine, probenecid, sulfinpyrazone: Possibly increased blood uric acid level and decreased antigout efficacy cyclosporine: Possibly decreased blood level and therapeutic effects of cyclosporine

Side Efect

CNS: Fever
GI: Anorexia, hepatotoxicity, nausea, vomiting
GU: Dysuria
HEME: Porphyria
MS: Arthralgia, gout, myalgia
SKIN: Acne, photosensitivity, pruritus, rash, urticaria

Cautions

Review liver function test results before and every 2 to 4 weeks during therapy.

Be aware that drug can affect the accuracy of certain urine ketone strip test results.

Because drug is metabolized by liver, monitor patient for evidence of hepatotoxicity, such as darkened urine, fever, jaundice, malaise, nausea, severe pain in feet or toes, and vomiting.

PATIENT SAFTY

Explain importance of complying with long-term pyrazinamide therapy.

Tell diabetic patient about possible changes in ketone measurement during therapy.

Instruct patient to report dark urine, fever, malaise, nausea, severe pain in feet or toes, vomiting, and yellowing of skin or eyes.

Inform patient of need for regular blood tests and follow-up visits with prescriber.

Urge patient to minimize exposure to sun and to wear protective clothing, hat, sunglasses, and sunscreen when outdoors.

Category

Chemical class: Bromide dimethylcarbamate
Therapeutic class: Antimyasthenic

Pregnancy category: Not rated

Indications

To treat symptoms of myasthenia gravis Adults and adolescents. 180 to 540 mg once or twice daily (at least 6 hr between doses). SYRUP, Adults and adolescents. Initial: 30 to 60 mg every 3 to 4 hr, adjusted as needed. Maintenance: 60 mg to 1.5 g daily. Children. 7 mg/kg daily in 5 or 6 divided doses. I.V. OR

IM

Adults and adolescents. 2 mg every 2 to 3 hr.
I.M.INJECTION Neonates of myasthenic mothers.0.05 to 0.15 mg/kg every 4 to 6 hr. To reverse the effects of neuromuscular blockers I.V. INJECTION Adults and adolescents. 10 to 20 mg after 0.6 to 1.2 mg of I.V. atropine has been given.
DOSAGE ADJUSTMENT Dosage possibly reduced for patients with renal impairment.

Mechanism of Action

Improves muscle strength compromised by myasthenia gravis or neuromuscular blockade by competing with acetylcholine for its binding site on acetylcholinesterase. This action potentiates the effects of acetylchopyridostigmine bromide 883 P line on skeletal muscle and the GI tract. Inhibited destruction of acetylcholine allows freer transmission of nerve impulses across the neuromuscular junction. Route Onset Peak Duration P.O. 30–45 min 1–2 hr 3–6 hr P.O.() 30–60 min 1–2 hr 6–12 hr I.V. 2–5 min Unknown 2–4 hr I.M. 15 min Unknown 2–4 hr

Contraindications

Hypersensitivity to pyridostigmine or its components, mechanical obstruction of GI or urinary tract

Interactions

aminoglycosides (systemic), anesthetics (hydrocarbon inhalation), capreomycin, lidocaine (I.V.), lincomycins, polymyxins, quinine: Possibly antagonized effect of pyridostigmine on skeletal muscle; possibly decreased neuromuscular blocking activity of these (with large doses of pyridostigmine) anesthetics (local): Inhibited neuronal transmission, increased anesthesia effects anticholinergics: Possibly masked pyridostigmine overdose; reduced intestinal motility
cholinesterase inhibitors: Increased risk of additive toxicity edrophonium: Possibly worsening of status guanadrel, guanethidine, mecamylamine, neuromuscular blockers, procainamide: Possibly prolonged phase I blocking effect or reversal of nondepolarization blockade quinidine, trimethaphan: Possibly antagonized effects of pyridostigmine

Side Efect

EENT: Increased salivation, lacrimation, miosis
GI: Abdominal cramps, diarrhea, increased peristalsis, nausea, vomiting
GU: Urinary frequency, incontinence, or urgency
MS: Fasciculations, muscle spasms or weakness
RESP: Increased tracheobronchial secretions
SKIN: Diaphoresis

Cautions

Use pyridostigmine cautiously in patients with renal disease because drug is mainly excreted unchanged by kidneys. Monitor BUN and serum creatinine levels.
WARNING Maintain a rigid dosing schedule because a missed or late dose can precipitate myasthenic crisis.

Observe for cholinergic reactions when administering drug I.V. or I.M.
WARNING Pyridostigmine overdose may obscure diagnosis of myasthenic crisis because main symptom in both is muscle weakness. Treat cholinergic crisis by stopping anticholinesterase, giving atropine as prescribed, and helping with endotracheal intubation and mechanical ventilation, if needed.

Be aware that reversal of neuromuscular blockade usually occurs in 15 to 30 minutes. Be prepared to maintain patent airway and ventilation until normal voluntary respiration returns completely. Assess respiratory measurements and muscle tone with peripheral nerve stimulator device, as indicated.

PATIENT SAFTY

Instruct patient to take pyridostigmine as directed and on schedule. Explain that a late or missed dose can precipitate a crisis. Suggest the use of a battery-operated alarm clock as a reminder.

Tell patient to take drug with a full glass of water or with food or milk if GI distress occurs.

Warn patient not to crush or chew tablets.

Ask patient to record pyridostigmine dosage, times taken, and drug effects to help determine optimal dosage and schedule.

Urge patient to carry medical identification describing her condition and drug regimen.

Category

Chemical class: Benzodiazepine
Therapeutic class: Sedative-hypnotic

Pregnancy category: X

Controlled substance schedule: IV

Indications

To treat insomnia
Adults. 15 mg at bedtime.
DOSAGE ADJUSTMENT In elderly and debilitated patients, dosage may be reduced to 7.5 mg at bedtime after 1 or 2 nights of therapy.

Mechanism of Action

May antagonize mu receptors at limbic, thalamic, and hypothalamic regions of the brain, blocking release of such inhibitory neurotransmitters as gamma-aminobutyric acid (GABA) and acetylcholine. Central receptors interact with GABA receptors, allowing for greater influx of chloride into the neuron, thereby suppressing neuronal excitability. GABA effects may inhibit spinal afferent pathways and block the cortical and limbic arousal that normally occurs when reticular pathways are stimulated. These effects result in various levels of CNS depression, including sleep.

Contraindications

Hypersensitivity to quazepam or its components, pregnancy, sleep apnea (known or suspected)

Interactions

addictive : Possibly habituation carbamazepine: Decreased blood quazepam level, possibly increased blood carbamazepine level cimetidine, diltiazem, disulfiram, erythromycin, fluoxetine, fluvoxamine, isoniazid, itraconazole, ketoconazole, nefazodone, oral contraceptives, propoxyphene, ranitidine, verapamil: Possibly potentiated effects of quazepam clozapine: Possibly syncope, with respiratory depression or arrest CNS depressants, tricyclic antidepressants: Increased CNS depression CYP2B6 substrates such as bupropion and efavirenz: Possibly increased plasma levels of these agents leading to increased risk of adverse effects digoxin: Possibly increased blood digoxin level and risk of digitalis toxicity levodopa: Possibly decreased therapeutic effects of levodopa
phenytoin: Increased risk of phenytoin toxicity theophyllines: Possibly antagonized effects of quazepam zidovudine: Increased risk of zidovudine toxicity grapefruit juice: Increased quazepam level
alcohol use: Additive CNS depression smoking: Possibly decreased effectiveness of quazepam

Side Efect

CNS: Abnormal complex behaviors, such as sleep driving; amnesia (anterograde); anxiety; ataxia; confusion; depression; dizziness; drowsiness; euphoria; fatigue; headache; light-headedness; paresthesia; slurred speech; suicidal ideation; tremor; weakness
CV: Chest pain, palpitations, tachycardia
EENT: Blurred vision, dry mouth, hyperacusis, photophobia, throat tightness, worsening of glaucoma
GI: Abdominal cramps, constipation, diarrhea, heartburn, nausea, thirst, vomiting
GU: Renal dysfunction, urinary incontinence, urine retention
MS: Muscle spasms
RESP: Dyspnea, increased tracheobronchial secretions
Other: Anaphylaxis, angioedema

Cautions

Use quazepam cautiously in patients with angle-closure glaucoma because of drug’s anticholinergic effects; in patients with hepatic dysfunction because this condition may prolong quazepam’s half-life; in patients with myasthenia gravis because drug may worsen condition; in patients with severe COPD because adverse effects of quazepam may compromise respiratory function; in patients with renal dysfunction because accumulation of metabolites may result in toxicity; and in elderly patients because of age-related decreases in hepatic, renal, and cardiac function.
WARNING Monitor patient closely for signs and symptoms of hypersensitivity reactions, such as dyspnea, throat tightness, nausea, vomiting, and swelling. If present, discontinue quazepam immediately, notify prescriber, and provide supportive care.
WARNING Notify prescriber if eye pain develops in patient with angle-closure glaucoma.
WARNING Be aware that quazepam may intensify signs and symptoms of depression. Monitor patient closely for evidence of suicidal ideation, and institute suicide precautions, as needed.

PATIENT SAFTY

Instruct patient to stop taking quazepam and seek emergency care if she has trouble breathing, throat tightness, nausea, vomiting, or abnormal swelling.

Advise patient that drug may cause abnormal behaviors during sleep, such as driving a car, eating, talking on the phone, or having sex without recall of the event. If family members notice such behavior, or if patient sees evidence of it upon awakening, prescriber should be notified.

Urge patient to avoid consuming alcohol during quazepam therapy because sedation and risk of abnormal behaviors, such as sleep driving, may increase.

Instruct patient not to stop drug abruptly after prolonged use (6 weeks or more).

Instruct female patient of childbearing age to use effective contraception during therapy and to notify prescriber immediately of known or suspected pregnancy.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes.

Category

Chemical class: Dibenzothiazepine derivative
Therapeutic class: Antipsychotic

Pregnancy category: C

Indications

To treat schizophrenia
Adults. Initial: 25 mg b.i.d. on day 1. Increased by 25 to 50 b.i.d. or t.i.d. on days 2 and 3. Usual: 300 to 400 mg daily by day 4, in divided doses b.i.d. or t.i.d. Increased every 2 days in increments of 25 to 50 mg b.i.d., as needed. Maximum: 800 mg daily.
Adults. Initial: 300 mg once daily in evening. Dosage increased daily in increments up to 300 mg, as needed. Maximum: 800 mg daily. To manage psychotic disorders other than schizophrenia
Adults. Initial: 25 mg b.i.d. on day 1. Dosage increased by 25 to 50 mg b.i.d. or t.i.d. on days 2 and 3. Usual: 300 to 400 mg daily by day 4, in divided doses b.i.d. or t.i.d. Dosage increased every 2 days in increments of 25 to 50 mg b.i.d., as needed. Maximum: 800 mg daily. To treat depressive episodes in bipolar disorder
Adults. Initial: On day one, 50 mg once at bedtime; day two, 100 mg once at bedtime; day three, 200 mg once at bedtime; day four, 300 mg once at bedtime. Maintenance: 300 mg once daily at bedtime.
Adults. Initial: 50 mg once daily in evening on day 1, followed by 100 mg once daily in evening on day 2, 200 mg once daily in evening on day 3, and 300 mg once daily in evening on day 4 and thereafter. As adjunct therapy with antidepressants to treat major depressive disorder
Adults. Initial: 50 mg once daily in evening, increased to 150 mg once daily in evening on day 3. Maximum: 300 mg daily in evening. To treat acute manic episodes in bipolar I disorder
Adults. 50 mg b.i.d., increased to 200 mg b.i.d on day 4 (in increments no greater than 100 mg daily) and then further increased to 400 mg b.i.d. on day 6 (in increments no greater than 200 mg daily), as needed. To treat acute manic episodes in bipolar I disorder as monotherapy; as adjunct with lithium or divalproex to treat acute manic episodes in bipolar I disorder
Adults. Initial: 300 mg once daily in evening on day 1, followed by 600 mg once daily in evening on day 2 and 200 to 400 mg b.i.d. on day 3 and thereafter. Maintenance: 200 to 400 mg b.i.d.
DOSAGE ADJUSTMENT For elderly patients and patients with hepatic impairment, initial dosage no higher than 50 mg once daily and increased in increments of 50 mg/day depending on response and tolerance.

Mechanism of Action

May produce antipsychotic effects by interfering with dopamine binding to dopamine type 2 (D2)-receptor sites in the brain and by antagonizing serotonin 5-HT2, dopamine type 1 (D1), histamine H1, and adrenergic alpha1and alpha2receptors.

Contraindications

Hypersensitivity to quetiapine or its components

Interactions

antihypertensives: Possibly enhanced antihypertensive effects of these cimetidine, erythromycin, fluconazole, itraconazole,
ketoconazole: Decreased clearance and possibly increased effects of quetiapine
CNS depressants: Possibly increased CNS depression lorazepam: Possibly increased effects of lorazepam phenytoin, thioridazine: Increased clearance and possibly decreased effectiveness of quetiapine
alcohol use: Possibly enhanced CNS depression

Side Efect

CNS: Depression, dizziness, drowsiness, dystonia, extrapyramidal reactions, hypertonia, lethargy, restless leg syndrome, somnolence, suicidal ideation, tardive dyskinesia
CV: Cardiomyopathy, hypercholesterolemia, myocarditis, orthostatic hypotension, palpitations
EENT: Dry mouth, nasal congestion, pharyngitis, rhinitis
ENDO: Hyperglycemia, syndrome of inappropriate ADH secretion
GI: Anorexia, constipation, indigestion
HEME: Agranulocytosis, leukopenia, neutropenia
MS: Dysarthria, muscle weakness, rhabdomyolysis
RESP: Cough, dyspnea
SKIN: Diaphoresis, Stevens-Johnson syndrome
Other: Anaphylaxis, flulike symptoms, weight gain

Cautions

WARNING Quetiapine shouldn’t be used for elderly patients with dementia-related psychosis because drug increases the risk of death in these patients.

Monitor patients (particularly young adults) closely for suicidal tendencies, especially when therapy starts or dosage changes, because depression may worsen temporarily during these times.
WARNING Monitor patient taking quetiapine for predisposing factors for neuroleptic malignant syndrome, such as heat stress, physical exhaustion, dehydration, and organic brain disease. Neuroleptic malignant syndrome includes hyperpyrexia, muscle rigidity, altered mental status, and autonomic instability (which may include irregular pulse or blood pressure, tachycardia, diaphoresis, and arrhythmias).

Monitor patient for signs of tardive dyskinesia, a potentially irreversible complication characterized by involuntary, dyskinetic movements of tongue, mouth, jaw, eyelids, or face. Notify prescriber if such signs develop because quetiapine therapy may need to be stopped.

Monitor patient for orthostatic hypotension, especially during initial dosage titration period. Be prepared to correct underlying conditions, such as hypovolemia and dehydration, before starting quetiapine therapy, as prescribed.

Monitor patient for prolonged abnormal muscle contractions, especially during the first few days of quetiapine therapy, in male patients, and in younger patients.

Assess patient for hypothyroidism because drug can cause dose-dependent decreases in total and free thyroxine (T4) levels.

Monitor laboratory results during first 3 weeks of therapy for transient elevations in hepatic enzyme levels. Notify prescriber if they persist or worsen.

Monitor patient’s blood glucose and lipid levels routinely, as ordered, because drug increases the risk of hyperglycemia and hypercholesterolemia.

Check CBC often during the first few months of therapy, as ordered, in patients with a low white blood cell count or a history of drug-induced hematologic problems. If counts drop or patient develops a fever or other signs of infection, notify prescriber and expect to discontinue drug and provide supportive care.

PATIENT SAFTY

Instruct patient to take quetiapine with food to reduce stomach upset.

Advise patient not to stop taking quetiapine suddenly because doing so may exacerbate his symptoms.

Inform patient that quetiapine therapy may cause dizziness or drowsiness. Advise him not to drive or perform other activities that require alertness until drug’s full CNS effects are known.

Instruct patient to rise slowly from a seated or lying position to reduce the risk of dizziness or fainting.

Caution patient to avoid consuming alcoholic beverages because they can increase dizziness and drowsiness.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes and particularly if patient is a young adult.

Encourage patient on long-term therapy to have regular eye examinations so that cataracts can be detected.

Category

Chemical class: Ethylester of quinaprilat
Therapeutic class: Antihypertensive

Pregnancy category: C

(first trimester), D (later trimesters)

Indications

To treat hypertension
Adults. Initial: 10 or 20 mg daily, adjusted every 2 wk based on clinical response. Maintenance: 20 to 80 mg daily or in divided doses b.i.d.
DOSAGE ADJUSTMENT Initial dosage reduced to 5 mg daily for patients who are dehydrated from previous diuretic therapy, those who are still receiving diuretic therapy, and those with creatinine clearance of 30 to 60 ml/min/1.73 m2. Dosage reduced to 2.5 mg daily for patients with creatinine clearance of 10 to 30 ml/min/1.73 m2. Route Onset Peak Duration P.O. In 1 hr 2–4 hr Up to 24 hr

Mechanism of Action

Blocks conversion of angiotensin I to angiotensin II, leading to vasodilation, and reduces aldosterone secretion, which prevents water retention. Quinapril also reduces peripheral arterial resistance. These combined actions lead to a reduction in blood pressure.

Contraindications

History of angioedema related to previous treatment with ACE inhibitor, hypersensitivity to quinapril or its components

Interactions

allopurinol, bone marrow depressants, corticosteroids (systemic), procainamide: Increased risk of fatal neutropenia or agranulocytosis CNS depressants, other hypotension-producing : Additive hypotensive effects cyclosporine, potassium preparations, potassium-sparing diuretics: Possibly hyperkalemia lithium: Possibly increased blood lithium level and risk of toxicity NSAIDs, sympathomimetics: Decreased antihypertensive effect of quinapril sodium aurothiomalate: Possibly nitritoid reactions such as facial flushing, nausea, vomiting, and hypotension tetracyclines: Reduced tetracycline absorption low-salt milk, salt substitutes: Increased risk of hyperkalemia
alcohol use: Additive hypotensive effects

Side Efect

CNS: Depression, dizziness, drowsiness, fatigue, fever, headache, insomnia, lightheadedness, malaise, paresthesia, sleep disturbance, syncope, vertigo
CV: Chest pain, hypotension, orthostatic hypotension, palpitations, tachycardia
EENT: Amblyopia, dry mouth, loss of taste, pharyngitis
GI: Abdominal pain, constipation, diarrhea, indigestion, nausea, vomiting
GU: Impotence
MS: Arthralgia, back pain, myalgia
RESP: Cough, dyspnea
SKIN: Alopecia, diaphoresis, flushing, photosensitivity, pruritus, rash, urticaria
Other: Anaphylaxis, angioedema

Cautions

Use quinapril cautiously in patients with renal impairment.
WARNING Patients with heart failure, hyponatremia, or severe volume or salt depletion; those who’ve recently received intensive diuresis or an increase in diuretic dosage; and those undergoing dialysis may be at risk for excessive hypotension. Monitor blood pressure often for first 2 weeks of therapy and whenever quinapril or diuretic dosage increases. If excessive hypotension occurs, notify prescriber immediately, place patient in a supine position, and, if prescribed, infuse normal saline solution.
WARNING Because of the risk of angioedema, be prepared to discontinue drug and administer emergency measures, including subcutaneous epinephrine 1:1,000 (0.3 to 0.5 ml), if swelling of tongue, glottis, or larynx causes airway obstruction.

Monitor blood pressure often to assess drug’s effectiveness.

PATIENT SAFTY

Instruct patient to notify prescriber immediately and stop taking quinapril if he has swelling of the face, eyes, lips, or tongue or difficulty breathing.

Explain that drug may cause dizziness and light-headedness, especially for first few days of therapy. Advise patient to avoid hazardous activities until drug’s CNS effects are known and to notify prescriber if he faints.

Inform woman of childbearing age of risks of taking quinapril during pregnancy, especially during the second and third trimesters. Caution her to use effective contraception and to notify prescriber immediately of known or suspected pregnancy.

Advise patient having surgery or anesthesia to tell specialist that he takes quinapril.

Instruct patient to consult prescriber before using potassium supplements or salt substitutes that contain potassium.

Category

Chemical class: Dextrorotatory isomer of quinine
Therapeutic class: Class IA antiarrhythmic

Pregnancy category: C

Indications

To prevent or treat cardiac arrhythmias, including established atrial fibrillation, atrial flutter, paroxysmal atrial fibrillation, paroxysmal atrial tachycardia, paroxysmal atrioventricular junctional rhythm, paroxysmal ventricular tachycardia not associated with complete heart block, and premature atrial and ventricular contractions (QUINIDINE GLUCONATE)
Adults. 324 to 660 mg every 8 to 12 hr. Maximum: 1,944 mg daily. (QUINIDINE SULFATE)
Adults. 300 to 600 mg every 8 to 12 hr.
Adults. Initial: 325 mg every 2 to 3 hr for 5 to 8 doses, gradually increasing dosage as needed and prescribed. Maintenance: 325 to 488 mg t.i.d. or q.i.d. (QUINIDINE POLYGALACTURONATE)
Adults. Initial: 275 to 825 mg every 3 to 4 hr for 3 or 4 doses, then increased by 137.5 to 275 mg every 3rd or 4th dose until rhythm is restored or toxic effects occur. Maintenance: 275 mg b.i.d. or t.i.d. (QUINIDINE SULFATE)
Adults. Initial: For premature atrial and ventricular contractions, 200 to 300 mg t.i.d. or q.i.d.; for paroxysmal supraventricular tachycardia, 400 to 600 mg every 2 to 3 hr until terminated; for atrial flutter, individual titration after digitalization; for conversion of atrial fibrillation, 200 mg every 2 to 3 hr for 5 to 8 doses, followed by subsequent daily increases, as needed. Maintenance: 200 to 400 mg t.i.d. or q.i.d. Children. 6 mg/kg 5 times daily.
IV:(QUINIDINE GLUCONATE)
Adults. 800 mg in 40 ml of D5W at up to 0.25 mg/kg/min.
I.M.INJECTION(QUINIDINE SULFATE)
Adults. 190 to 380 mg every 2 to 4 hr. Maximum: 3 g daily. Route Onset Peak Duration P.O. Unknown Unknown 6–8 hr P.O.() Unknown Unknown 12 hr

Mechanism of Action

Depresses excitability, conduction velocity, and contractility of the myocardium and increases the effective refractory period, thus suppressing arrhythmic activity in the atria, ventricles, and His-Purkinje system.

Contraindications

Digitalis toxicity; history of quinidineinduced thrombocytopenic purpura or torsades de pointes; hypersensitivity to quinidine, other cinchona derivatives, or their components; long-QT syndrome; myasthenia gravis; pacemaker-dependent conduction disturbances

Interactions

antiarrhythmics, phenothiazines, rauwolfia alkaloids: Additive cardiac effects anticholinergics: Possibly intensified atropine-like adverse effects antimyasthenics: Antagonized antimyasthenic effects on skeletal muscle barbiturates,
rifampin: Possibly accelerated elimination and decreased effectiveness of quinidine
cimetidine: Increased elimination half-life, possibly leading to quinidine toxicity digoxin: Possibly digitalis toxicity hepatic enzyme inducers: Possibly decreased blood quinidine level neuromuscular blockers: Possibly potentiated neuromuscular blockade oral anticoagulants: Additive hypoprothrombinemia, increased risk of bleeding pimozide: Risk of arrhythmias quinine: Increased risk of quinidine toxicity urinary alkalizers (such as antacids, carbonic anhydrase inhibitors, citrates, sodium bicarbonate, thiazide diuretics): Increased renal tubular reabsorption of quinidine, possibly leading to quinidine toxicity verapamil: Possibly AV block, bradycardia, pulmonary edema, significant hypotension, and ventricular tachycardia

Side Efect

CNS: Anxiety, asthenia, ataxia, confusion, delirium, difficulty speaking, dizziness, drowsiness, extrapyramidal reactions, fever, headache, hypertonia, syncope, vertigo
CV: Complete heart block, orthostatic hypotension, palpitations, peripheral edema, prolonged QT interval, torsades de pointes, vasculitis, ventricular arrhythmias, widening QRS complex
EENT: Blurred vision, change in color perception, diplopia, dry mouth, hearing loss (high-frequency), pharyngitis, photophobia, rhinitis, tinnitus
GI: Abdominal pain, anorexia, constipation, diarrhea, indigestion, nausea, vomiting
HEME: Agranulocytosis, hemolytic anemia, leukopenia, neutropenia, thrombocytopenia, thrombocytopenic purpura
MS: Arthralgia, myalgia
RESP: Dyspnea
SKIN: Diaphoresis, eczema, exfoliative dermatitis, flushing, hyperpigmentation, photosensitivity, pruritus, psoriasis, purpura, rash, urticaria
Other: Angioedema, flulike symptoms, weight gain

Cautions

Give I.M. form of quinidine undiluted.

For intermittent I.V. infusion, dilute drug in 40 ml of D5W and administer using an infusion pump at a rate of 0.25 mg/kg/ min or less. Rapid administration may cause hypotension. Monitor ECG tracings and blood pressure throughout administration.

Monitor therapeutic blood level of quinidine, as ordered.

Monitor heart rate and rhythm closely because quinidine may cause serious

Side Efect

and can be cardiotoxic, especially at dosages exceeding 2.4 g daily. Implement continuous cardiac monitoring, as ordered.

Assess for early signs and symptoms of cinchonism, including blurred vision, change in color perception, confusion, diplopia, headache, and tinnitus, which may indicate quinidine toxicity.

PATIENT SAFTY

Advise patient to take quinidine at the same times every day and at evenly spaced intervals.

Instruct patient to swallow tablets whole, with a full glass of water, preferably while sitting upright.

Advise patient to take drug with food if GI upset occurs.

Urge patient to inform prescriber immediately of blurred or double vision, change in color perception, confusion, diarrhea, fever, headache, loss of hearing, or tinnitus.

Category

Chemical class: Cinchona alkaloid
Therapeutic class: Antimalarial

Pregnancy category: X

Indications

As adjunct to treat chloroquine-resistant malaria caused by Plasmodium falciparum ,
Adults. 600 to 650 mg every 8 hr for at least 3 days with one of the following: 250 mg of tetracycline every 6 hr for 7 days; 1.5 g of sulfadoxine and 75 mg of pyrimethamine combined as a single dose; 900 mg of clindamycin every 8 hr for 3 days; or 100 mg of doxycycline every 12 hr for 7 days. Children over age 8. 8.3 mg/kg every 8 hr for at least 3 days with one of the following: 5 mg/kg of tetracycline every 6 hr for 7 days; 6.7 to 13.3 mg/kg of clindamycin every 8 hr for 3 days; or 1.25 mg/kg of pyrimethamine and 25 mg/kg of sulfadoxine combined as a single dose.

Mechanism of Action

May disrupt function in malarial parasite by elevating intracellular pH in parasitic acid vesicles.

Contraindications

G6PD deficiency, history of quinineinduced blackwater fever or thrombocytopenic purpura, hypersensitivity to quinine or its components, optic neuritis, pregnancy, tinnitus

Interactions

acetazolamide, sodium bicarbonate: Increased risk of quinine toxicity aluminum-containing antacids: Possibly delayed or decreased quinine absorption aminophylline,
theophylline: Possibly increased quinine adverse effects antimyasthenics: Possibly antagonized antimyasthenic effect on skeletal muscle astemizole, cisapride, halofantrine, mefloquine, pimozide, quinidine, terfenadine: Increased risk of prolonged QT interval atorvastatin: Increased blood atorvastatin level; increased risk of myopathy or rhabdomyolysis carbamazepine, phenobarbital,
phenytoin: Possibly increased blood level of these ; possibly decreased blood quinine level
cimetidine: Possibly reduced quinine clearance debrisoquine, desipramine, dextromethorphan, flecainide, metoprolol, paroxetine: Possibly increased bood levels of these ; increased risk of

Side Efect

digoxin: Increased blood digoxin level erythromycin, ketoconazole, troleandomycin: Possibly increased blood quinine level hemolytics, neurotoxic , ototoxic : Increased risk of toxicity of these hepatic enzyme inducers,
rifampin: Possibly decreased blood quinine level mefloquine: Increased risk of seizures neuromuscular blockers: Potentiated neuromuscular blockade oral anticoagulants: Possibly increased anticoagulant effects and risk of bleeding

Side Efect

CNS: Headache
EENT: Blurred vision, hearing loss, tinnitus, vision changes
ENDO: Hypoglycemia
GI: Abdominal or epigastric pain, diarrhea, nausea, vomiting
HEME: Thrombocytopenia

Cautions

Be aware that quinine shouldn’t be used in patients with blackwater fever, which can follow chronic malaria, because they’re at increased risk for anemia and hemolysis with renal failure. Quinine also isn’t recommended for treating or preventing nocturnal leg cramps because life-threatening hematologic reactions have occurred with potential for chronic renal impairment.

Be aware that quinine shouldn’t be given I.M. Doing so may cause bleeding, bruising, or hematomas because of quinine’s effect on platelets.

Monitor patient with type 2 diabetes mellitus for alterations in blood glucose level because quinine stimulates release of insulin and may promote hypoglycemia.

Be aware that quinine can exacerbate optic neuritis or tinnitus. It may also exacerbate muscle weakness and cause dysphagia and respiratory distress in myasthenic patients.

Assess for early signs and symptoms of cinchonism, including blurred vision, confusion, diplopia, fever, headache, loss of hearing, and tinnitus, which may indicate quinine toxicity.

Be aware that patients who develop quinine-dependent antibodies could develop thrombocytopenia more rapidly and more severely upon re-exposure to quinine from any source.

PATIENT SAFTY

Instruct patient not to crush or chew quinine tablets; they taste bitter and can irritate the mouth and throat.

Advise patient to take drug with food or after meals to minimize GI irritation.

Urge patient to notify prescriber immediately if he experiences blurred or double vision, confusion, fever, headache, loss of hearing, or tinnitus, which are indicators of quinine toxicity.

Advise patient to avoid hazardous activities until he knows how quinine affects him.

Category

Chemical class: Substituted benzimidazole
Therapeutic class: Antiulcer

Pregnancy category: B

Indications

To provide short-term treatment of erosive esophagitis or ulcerative gastroesophageal reflux disease (GERD) DELAYED-RELEASE
Adults. For mild to moderate disease, 20 mg daily for 4 to 8 wk; course may be repeated if healing has not occurred at the end of 8 wk. For severe reflux with ulceration or stricture formation, 40 mg daily for 4 to 8 wk. To treat symptomatic GERD DELAYED-RELEASE Adults and adolescents age 12 and over. 20 mg daily for 4 wk. Course may be repeated if symptoms aren’t completely resolved. To provide maintenance treatment of erosive esophagitis or GERD DELAYED-RELEASE
Adults. 20 mg daily. To promote healing of duodenal ulcer, as adjunct to treat Helicobacter pylori–positive duodenal ulcer DELAYED-RELEASE
Adults. 20 mg daily after breakfast for up to 4 wk for ulcer healing and 2 wk when used with antibiotic therapy for H. pylori. As adjunct to reduce the risk of duodenal ulcer recurrence by eradicating H. pylori DELAYED-RELEASE
Adults. 20 mg b.i.d with morning and evening meals in conjunction with amoxirabeprazole sodium 892 cillin 1000 mg b.i.d for 7 days and clarithromycin 500 mg b.i.d. for 7 days. To treat hypersecretory conditions, such as Zollinger-Ellison syndrome DELAYED-RELEASE
Adults. Initial: 60 mg daily; may be increased, if needed, to 100 mg daily or 60 mg b.i.d.
DOSAGE ADJUSTMENT Dosage reduction may be needed in severe hepatic dysfunction.

Mechanism of Action

Decreases gastric acid secretion by suppressing its release at the secretory surface of gastric parietal cells. Rabeprazole also increases gastric pH and decreases basal acid output, which helps to heal ulcerated areas. In gastric parietal cells, it’s transformed to an active sulfonamide, which increases the clearance rate of Helicobacter pylori.

Contraindications

Hypersensitivity to rabeprazole, other substituted benzimidazoles (omeprazole, lansoprazole), or their components

Interactions

cyclosporine: Possibly inhibited cyclosporine metabolism digoxin: Increased risk of digitalis toxicity
warfarin: Possibly increased PT, INR

Side Efect

CNS: Coma, delirium, disorientation, dizziness, headache, malaise
GI: Abdominal pain, diarrhea, jaundice, nausea, vomiting
GU: Interstitial nephritis
HEME: Agranulocytosis, hemolytic anemia, leukopenia,pancytopenia,thrombocytopenia
MS: Rhabdomyolysis
RESP: Interstitial pneumonia
SKIN: Erythema multiforme, rash, StevensJohnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, angioedema, hyperammonemia

Cautions

Use rabeprazole cautiously in patients with hepatic dysfunction.

Expect to monitor serum gastrin level in long-term therapy to detect elevation.

Closely monitor Japanese men receiving rabeprazole for

Side Efect

because they’re more likely than other patients to have increased blood drug levels.

PATIENT SAFTY

Instruct patient to swallow delayed-release rabeprazole tablets whole.

Inform patients with hypersecretory conditions, such as Zollinger-Ellison syndrome, that treatment can last as long as 1 year.

Category

Chemical class: Benzothiophene derivative
Therapeutic class: Osteoporosis prophylactic

Pregnancy category: X

Indications

To prevent osteoporosis in postmenopausal women; to reduce risk of invasive breast cancer in postmenopausal women with osteoporosis; to reduce risk of invasive breast cancer in postmenopausal women at high risk
Adults. 60 mg daily.

Mechanism of Action

Prevents osteoporosis by binding to estrogen receptors, which decreases bone resorption and increases bone mineral density in postmenopausal women.

Contraindications

History of thromboembolic disease, hypersensitivity to raloxifene or its components, pregnancy

Interactions

ampicillin, cholestyramine: Decreased raloxifene absorption
warfarin: Possibly decreased PT

Side Efect

CNS: Depression, fever, insomnia, migraine, stroke
CV: Chest pain, hot flashes, peripheral edema, thromboembolism, thrombophlebitis
EENT: Laryngitis, pharyngitis, sinusitis
ENDO: Hot flashes
GI: Abdominal pain, cholelithiasis, flatulence, indigestion, nausea, vomiting
GU: Cystitis, infertility, leukorrhea, UTI, vaginitis
MS: Arthralgia, arthritis, leg cramps or spasms, myalgia
RESP: Cough, pneumonia, pulmonary embolism
SKIN: Diaphoresis, rash
Other: Flulike symptoms, weight gain

Cautions

Use cautiously in patients who smoke or have a history of stroke, TIA, atrial fibrillation, or hypertension because raloxifene may increase the risk of stroke.

Use cautiously in patients with renal impairment because effects of raloxifene on renal system are unknown.
WARNING Monitor patient’s limbs for impaired circulation and pain (possible thromboembolism).

Expect prescriber to stop drug at least 72 hours before and during periods of prolonged immobilization. Resume raloxifene therapy as prescribed after patient is fully ambulatory.

PATIENT SAFTY

Advise patient to avoid lengthy immobility during travel while taking raloxifene because of the increased risk of thromboembolism.

Instruct patient to report

Side Efect

to prescriber immediately, especially leg pain or swelling, sudden chest pain, shortness of breath, coughing up blood, or a sudden change in vision.

Stress the importance of compliance with long-term raloxifene therapy.

Advise patient that postmenopausal women require an average of 1,500 mg of elemental calcium and 400 to 800 international units of vitamin D daily.Vitamin D requirement is increased in women over age 70, women with GI malabsorption syndromes, and women who are chronically ill or nursing home bound. Review dietary sources of calcium and vitamin D, and have patient discuss supplements with prescriber, as needed.

Category

Chemical class: Melatonin receptor agonist
Therapeutic class: Hypnotic

Pregnancy category: C

Indications

To treat insomnia in patients having difficulty falling asleep
Adults. 8 mg 30 min before at bedtime. Route Onset Peak Duration P.O. Unknown 0.5–1.5 hr Unknown

Mechanism of Action

Binds to melatonin receptors MT1 and MT2 in the suprachiasmatic nucleus (SCN) of the hypothalamus. The SCN regulates the sleep-wake cycle, and endogenous melatonin probably is involved in maintaining the circadian rhythm underlying that cycle.

Contraindications

Concurrent therapy with fluvoxamine, history of angioedema with previous ramelteon treatment, hypersensitivity to ramelteon or its components, severe hepatic dysfunction

Interactions

benzodiazepines, melatonin, other sedativehypnotics: Possible additive sedative effects fluconazole, fluvoxamine,
ketoconazole: Increased plasma ramelteon levels
rifampin: Decreased ramelteon effectiveness
alcohol use: Possibly additive CNS effect

Side Efect

CNS: Agitation, amnesia, anxiety, bizarre behavior, complex behaviors such as sleep driving, depression, dizziness, fatigue, hallucinations, headache, insomnia exacerbation, mania, somnolence, suicidal ideation
EENT: Throat tightness
ENDO: Decreased testosterone level, increased prolactin level
GI: Diarrhea, dysgeusia, nausea, vomiting
MS: Arthralgia, myalgia
RESP: Dyspnea, upper respiratory tract ramelteon 894 infection
Other: Anaphylaxis, angioedema

Cautions

Be aware that ramelteon therapy is not recommended for patients with severe sleep apnea or COPD because its effects have not been studied in these patient populations.

Use cautiously in patients with mild to moderate hepatic dysfunction. Drug is contraindicated in severe hepatic dysfunction.

Ramelteon is the first approved hypnotic not classified as a controlled substance.
WARNING Monitor patient closely for hypersensitivity reactions such as dyspnea, throat tightness, nausea, vomiting, and swelling. If present, discontinue ramelteon immediately, notify prescriber, and provide supportive care.

Watch patient closely for suicidal tendencies, particularly when therapy starts and dosage changes, because depression may worsen temporarily during these times, possibly leading to suicidal ideation.

PATIENT SAFTY

Instruct patient not to take ramelteon with or immediately after eating a high-fat meal.

Caution patient to avoid potentially hazardous activities after taking ramelteon; drug’s intended effect is to decrease alertness.

Advise patient that drug may cause abnormal behaviors during sleep, such as driving a car, eating, talking on the phone, or having sex without any recall of the event. If family members notice any such behavior or patient sees evidence of such behavior upon awakening, prescriber should be notified.

Advise limiting alcohol during therapy.

Tell patient to notify prescriber if insomnia worsens or new signs or symptoms occur.

Inform patient that drug may affect reproductive hormones; urge patient to report cessation of menses or galactorrhea (females) or decreased libido or problems with infertility.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes.

Category

Chemical class: Ethylester of ramiprilat
Therapeutic class: Antihypertensive

Pregnancy category: C

(first trimester), D (later trimesters)

Indications

To treat heart failure after MI
Adults. Initial: 1.25 to 2.5 mg b.i.d. Maintenance: 5 mg b.i.d. To treat hypertension
Adults. Initial: 2.5 mg daily. Maintenance: 2.5 to 20 mg once daily or in divided doses b.i.d.
DOSAGE ADJUSTMENT Initial dosage reduced to 1.25 mg daily for patients dehydrated from diuretics, those receiving diuretics, and those with creatinine clearance less than 40 ml/min/1.73 m2; dosage then slowly increased until blood pressure is under control or maximum daily dose of 5 mg is reached. Route Onset Peak Duration P.O. 1–2 hr 4 –6.5 hr 24 hr

Mechanism of Action

Blocks conversion of angiotensin I to angiotensin II, causing vasodilation, and reduces aldosterone secretion, which prevents water retention. Ramipril also reduces peripheral arterial resistance. Combined, these actions reduce blood pressure.

Contraindications

Hypersensitivity to ramipril, its components, or any other ACE inhibitors

Interactions

allopurinol, bone marrow depressants, corticosteroids (systemic), procainamide: Increased risk of fatal neutropenia or agranulocytosis CNS depressants, other hypotensionproducing : Additive hypotensive effect cyclosporine, potassium preparations, potassium-sparing diuretics: Possibly hyperkalemia insulin, oral antidiabetics: Increased risk of hypoglycemia lithium: Increased risk of lithium toxicity NSAIDs, sympathomimetics: Decreased antihypertensive effect of ramipril sodium aurothiomalate: Increased risk of nitritoid reaction (facial flushing, nausea, vomiting, hypotension) telmisartan: Possibly increased risk of adverse effects, especially renal dysfunction tetracyclines: Reduced tetracycline absorption low-salt milk, salt substitutes: Increased risk of hyperkalemia
alcohol use: Additive hypotensive effects

Side Efect

CNS: Depression, dizziness, drowsiness, fatigue, fever, headache, insomnia, lightheadedness, malaise, paresthesia, sleep disturbance, syncope, vertigo
CV: Chest pain, hypotension, orthostatic hypotension, palpitations, tachycardia
EENT: Amblyopia, dry mouth, loss of taste, pharyngitis
GI: Abdominal pain, constipation, diarrhea, elevated liver function test results, hepatic failure, hepatitis, nausea, vomiting
GU: Acute renal failure, elevated BUN and serum creatinine levels, impotence, oliguria, progressive azotemia
HEME: Agranulocytosis, anemia, bone marrow depression, pancytopenia
MS: Arthralgia, back pain, myalgia
RESP: Cough, dyspnea
SKIN: Alopecia, diaphoresis, flushing, jaundice, onycholysis, pemphigoid, photosensitivity, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Angioedema

Cautions

Use ramipril cautiously in patients with renal or hepatic impairment.
WARNING Patients with dehydration, heart failure, or hyponatremia; those who’ve recently received intensive diuresis or an increase in diuretic dosage; and those having dialysis may risk excessive hypotension. Monitor such patients closely the first 2 weeks of therapy and whenever ramipril or diuretic dosage increases. If excessive hypotension occurs, notify prescriber immediately, place patient in a supine position, and, if prescribed, infuse normal saline solution.
WARNING Because of the risk of angioedema, be prepared to stop drug and provide emergency measures, including subcutaneous epinephrine 1:1,000 (0.3 to 0.5 ml), if swelling of tongue, glottis, or larynx causes airway obstruction.

Monitor blood pressure frequently during therapy to assess drug’s effectiveness.

Monitor patient’s renal and hepatic function closely during therapy.

PATIENT SAFTY

Advise patient to stop taking ramipril and inform prescriber immediately if she experiences swelling of the face, eyes, lips, or tongue or has difficulty breathing.

Explain that drug may cause dizziness and light-headedness, especially during first few days of therapy. Instruct patient to notify prescriber immediately if she faints.

Inform female patient of childbearing age of the risks of taking ramipril during pregnancy. Caution patient to use effective contraception and to report known or suspected pregnancy immediately.

Urge patient to tell providers that she takes ramipril before having surgery or anesthesia.

Tell patient to ask prescriber before using supplements or salt substitutes that contain potassium.

Category

Chemical class: Aminoalkyl-substituted furan derivative
Therapeutic class: Antiulcer agent, gastric acid secretion inhibitor

Pregnancy category: B

Indications

To prevent duodenal and gastric ulcers ranitidine hydrochloride 896 , EFFERVESCENT GRANULES, EFFERVESCENT , SYRUP, Adults and adolescents. 150 mg at bedtime. To provide short-term treatment of active duodenal and benign gastric ulcers , EFFERVESCENT GRANULES, EFFERVESCENT , SYRUP, Adults and adolescents. 150 mg b.i.d. for gastric ulcers; 150 mg b.i.d. or 300 mg at bedtime for duodenal ulcers. Children ages 1 month to 16 years. 2 to 4 mg/kg b.i.d. up to 300 mg daily. Maintenance: 2 to 4 mg/kg daily up to 150 mg daily. CONTINUOUS
IV: Adults and adolescents. 6.25 mg/hr. Maximum: 400 mg daily. INTERMITTENT
IV: Adults and adolescents. 50 mg diluted to total volume of 100 ml and infused over 15 to 20 min every 6 to 8 hr. Maximum: 400 mg daily. Children. 2 to 4 mg/kg daily diluted to a suitable volume and infused over 15 to 20 min.
I.V.INJECTION Adults and adolescents. 50 mg diluted to total volume of 20 ml and injected slowly over no less than 5 min every 6 to 8 hr. Maximum: 400 mg daily.
I.M.INJECTION Adults and adolescents. 50 mg every 6 to 8 hr. Maximum: 400 mg daily. To treat acute gastroesophageal reflux disease , EFFERVESCENT GRANULES, EFFERVESCENT , SYRUP, Adults and adolescents. 150 mg b.i.d. EFFERVESCENT Children ages 1 month to 16 years.2.5 to 5 mg/kg b.i.d. INTERMITTENT
IV: Children. 2 to 8 mg/kg diluted to suitable volume and infused over 15 to 20 min t.i.d. To treat erosive esophagitis , EFFERVESCENT GRANULES, EFFERVESCENT , SYRUP, Adults and adolescents. 150 mg q.i.d. EFFERVESCENT Children ages 1 month to 16 years. 2.5 to 5 mg/kg b.i.d. To treat hypersecretory GI conditions, such as Zollinger-Ellison syndrome, systemic mastocytosis, and multiple endocrine adenoma syndrome , EFFERVESCENT GRANULES, EFFERVESCENT , SYRUP, Adults and adolescents. Initial: 150 mg b.i.d., adjusted as needed. Maximum: 6 g daily in divided doses. CONTINUOUS
IV: Adults and adolescents. Initial: 1 mg/kg/hr, increased by 0.5 mg/kg/hr up to 2.5 mg/kg/ hr. Maximum: 400 mg daily. INTERMITTENT
IV:
Adults. 50 mg diluted to total volume of 100 ml and infused over 15 to 20 min every 6 to 8 hr. Maximum: 400 mg daily.
I.V.INJECTION Adults and adolescents. 50 mg diluted to total of 20 ml and injected slowly over at least 5 min every 6 to 8 hr. Maximum: 400 mg daily.
I.M.INJECTION
Adults. 50 mg every 6 to 8 hr. To prevent acid indigestion, heartburn, and sour stomach caused by eating certain or drinking certain beverages Adults and adolescents. 75 mg 30 to 60 min before food or beverages expected to cause symptoms. Maximum: 150 mg daily over no more than 2 continuous wk. To treat acid indigestion, heartburn, and sour stomach Adults and adolescents. 75 mg when symptoms start; repeated once within 24 hr, if needed.
DOSAGE ADJUSTMENT For patients whose creatinine clearance is less than 50 ml/min/ 1.73 m2, 150 mg P.O. every 24 hr with dosage interval increased thereafter to every 12 hr, as needed. Or 50 mg I.V. every 18 to 24 hr with dosage interval increased to every 12 hr, as needed. Dosage reduction may also be necessary for patients with hepatic dysfunction. Route Onset Peak Duration P.O., I.V., Unknown 1–3 hr 13 hr I.M.

Mechanism of Action

Inhibits basal and nocturnal secretion of gastric acid and pepsin by competitively inhibiting the action of histamine at H2 receptors on gastric parietal cells. This action reduces total volume of gastric juices and, thus, irritation of GI mucosa.

Contraindications

Acute porphyria, hypersensitivity to ranitidine or its components

Interactions

antacids: Decreased ranitidine absorption atazanavir, delavirdine, diazepam, gefitinib, itraconazole, ketoconazole, sucralfate: Decreased absorption of these bone marrow depressants: Increased risk of neutropenia or other blood dyscrasias glipizide, glyburide, metoprolol, midazolam, nifedipine, phenytoin, theophylline, triazolam: Increased effects of these , possibly leading to toxic reactions procainamide: Possibly increased risk of procainamide toxicity
warfarin: Possibly altered PT
alcohol use: Increased blood alcohol level (with oral ranitidine)

Side Efect

CNS: Dizziness, drowsiness, fever, headache, insomnia
CV: Vasculitis
GI: Abdominal distress, constipation, diarrhea, nausea, vomiting
GU: Acute interstitial nephritis, impotence
MS: Arthralgia, myalgia
RESP: Bronchospasm
SKIN: Alopecia, erythema multiforme, rash
Other: Anaphylaxis, angioedema

Cautions

Be aware that ranitidine must be diluted for I.V. use if not using premixed solution. For I.V. injection, dilute to total of 20 ml with normal saline solution, D5W, D10W, lactated Ringer’s solution, or 5% sodium bicarbonate. For I.V. infusion, dilute to total volume of 100 ml of same solutions.

Give I.V. injection at no more than 4 ml/ min, intermittent I.V. infusion at 5 to 7 ml/min, and continuous I.V. infusion at 6.25 mg/hr (except with hypersecretory conditions, when initial infusion rate is 1 mg/kg/hr, gradually increased after 4 hours, as needed, in increments of 0.5 mg/kg/hr).

Don’t add additives to premixed solution.

Stop primary I.V. solution infusion during piggyback administration.

PATIENT SAFTY

Tell patient to dissolve 150-mg effervescent tablets or granules in 6 to 8 oz water or 25-mg effervescent tablets in at least 5 ml water.

Advise patient (or parent) to wait until effervescent tablet is completely dissolved before taking (or giving to child or infant).

Caution patient not to chew effervescent tablets, swallow them whole, or let them dissolve on the tongue.

Alert patients with phenylketonuria that effervescent tablets and granules contain phenylalanine.

Tell patient that she may take drug with food.

Tell patient to stop taking ranitidine and contact prescriber if she has trouble swallowing, vomits blood, or passes black or bloody stools.

If needed, advise patient to take antacids, 2 hours before or after ranitidine; advise against taking other acid reducers with drug.

If patient takes drug to prevent heartburn, tell her to contact prescriber about frequent chest pain or wheezing with heartburn; stomach pain; unexplained weight loss; nausea; vomiting; heartburn lasting more than 3 months; heartburn with light-headedness, dizziness, or sweating; chest or shoulder pain with shortness of breath, sweating, light-headedness, or pain spreading to arms, neck, or shoulders. These problems may be serious.

Inform patient that healing of an ulcer may require 4 to 8 weeks of therapy.

Category

Chemical class: Piperazineacetamide
Therapeutic class: Antianginal

Pregnancy category: C

Indications

To treat chronic angina
Adults. Initial: 500 mg b.i.d., increased to 1,000 mg b.i.d., as needed. Maximum: 1,000 mg b.i.d.
DOSAGE ADJUSTMENT For patients taking a moderate CYP3A inhibitor, such as diltiazem or verapamil, maximum dosage reduced to 500 mg b.i.d. For patients taking cyclosporine, dosage reduced according to clinical response Route Onset Peak Duration P.O. Unknown 2–5 hr Unknown

Mechanism of Action

Exerts anti-ischemic and antianginal effects by an unknown mechanism not dependent on reductions in heart rate or blood pressure. Ranolazine inhibits cardiac late sodium current, but how this action inhibits angina symptoms is also unknown.

Contraindications

Hypersensitivity to ranolazine or its components, hepatic impairment, QT-interval prolongation, torsades de pointes, use of CYP3A inducers or strong inhibitors

Interactions

CYP3A inducers, such as carbamazepine, phenobarbital, phenytoin, rifabutin, rifampin, rifapentin,
St. John’s wort: Decreased blood ranolazine level and decreased effectiveness CYP3A substrates, such as cyclosporine: Possibly increased cyclosporine level CYP3A inhibitors, such as clarithromycin, diltiazem, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, verapamil: Increased blood ranolazine level and increased risk of

Side Efect

digoxin: Increased blood digoxin level

Side Efect

CNS: Asthenia, confusion, dizziness, headache, hypoesthesia, paresthesia, tremor, vertigo
CV: Bradycardia, hypotension, orthostatic hypotension, palpitations, peripheral edema, QT-interval prolongation
EENT: Blurred vision, dry mouth, tinnitus
GI: Abdominal pain, constipation, nausea, vomiting
GU: Elevated creatinine level, hematuria, renal failure
HEME: Eosinophilia, leukopenia, pancytopenia, thrombocytopenia
RESP: Dyspnea, pulmonary fibrosis
Other: Angioedema

Cautions

Monitor patient’s QT interval, as ordered, because ranolazine prolongs it in a doserelated manner.

Assess effectiveness of ranolazine at preventing anginal pain.

Monitor patient’s serum creatinine, BUN, magnesium, potassium, and liver enzyme levels.

PATIENT SAFTY

Instruct patient to take ranolazine exactly as prescribed.

Inform patient that drug may be taken with or without food.

Caution patient to swallow tablets whole and not to crush, break, or chew them.

Advise patient to limit the amount of grapefruit and grapefruit juice consumed while taking this drug.

Advise patient to notify prescriber if serious or persistent

Side Efect

occur.

Category

Chemical class: Propargylamine
Therapeutic class: Irreversible MAO inhibitor

Pregnancy category: C

Indications

To treat idiopathic Parkinson’s disease as initial monotherapy in early-stage disease
Adults. 1 mg once daily. As adjunct with levodopa or levodopa and carbidopa in treatment of laterstage idiopathic Parkinson’s disease
Adults. 0.5 mg once daily increased to 1 mg once daily, as needed.
DOSAGE ADJUSTMENT For patients with mild hepatic failure, dosage shouldn’t exceed 0.5 mg daily.

Mechanism of Action

Inhibits metabolic degradation of catecholamines and serotonin in the CNS and peripheral tissues, increasing extracellular dopamine level in the striatum. The increased dopamine level helps control alterations in voluntary muscle movement (such as tremors and rigidity) in Parkinson’s disease because dopamine, a neurotransmitter, is essential for normal motor function. By stimulating peripheral and central dopaminergic 2 (D2) receptors on postsynaptic cells, dopamine inhibits firing of striatal neurons (such as cholineric neurons), improving motor function. Route Onset Peak Duration P.O. Unknown 1 hr Unknown

Contraindications

Acute MI; angina; cardiac arrhythmias; coronary artery disease; cerebrovascular disease; elective surgery that requires general anesthesia; hypersensitivity to rasagiline or its components; pheochromocytoma; moderate to severe hepatic impairment; stroke; use within 14 days of cyclobenzaprine, dextromethorphan, MAO inhibitors, meperidine, mirtazapine, tramadol, methadone, propoxyphene, St. John’s wort, or sympathomimetic amines

Interactions

ciprofloxacin and other CYP1A2 inhibitors: Increased rasagiline plasma level dextromethorphan: Increased risk of psychosis or bizarre behavior levodopa, levodopa and carbidopa: Increased risk of dyskinesias MAO inhibitors, sympathomimetics: Increased risk of hypertensive crisis meperidine, methadone, propoxyphene, tramadol: Increased risk of life-threatening

Side Efect

characterized by coma, severe hypertension or hypotension, severe respiratory depression, seizures, malignant hyperpyrexia, excitation, and peripheral vascular collapse selective serotonin reuptake inhibitors, tetracyclic antidepressants, tricyclic antidepressants: Increased risk of severe CNS toxicity with hyperpyrexia, behavioral and mental status changes, diaphoresis, muscle rigidity, hypertension, syncope, and possible death

Side Efect

CNS: Abnormal dreams, amnesia, anxiety, asthenia, ataxia, cerebral ischemia, coma, confusion, depression, difficulty thinking, dizziness, dyskinesia, dystonia, fever, hallucinations, headache, malaise, manic depressive reaction, nightmares, paresthesia, seizures, somnolence, stroke, stupor, syncope, vertigo
CV: Angina, bundle branch heart block, chest pain, heart failure, MI, hypertensive crisis, postural hypotension, thrombophlebitis, ventricular tachycardia or fibrillation
EENT: Blurred vision, conjunctivitis, dry mouth, gingivitis, hemorrhage, laryngeal edema, retinal detachment or hemorrhage, rhinitis
GI: Abdominal pain, anorexia, constipation, diarrhea, dyspepsia, dysphagia, epistaxia, gastroenteritis, gastrointestinal hemorrhage, intestinal obstruction or perforation, liver function test abnormalities, nausea, vomiting
GU: Acute renal failure, albuminuria, decreased libido, hematuria, impotence, incontinence, priapism
HEME: Anemia, leukopenia, thrombocytopenia
MS: Arthralgia, arthritis, bone necrosis, bursitis, leg cramps, myasthenia, neck pain or stiffness, tenosynovitis
RESP: Apnea, asthma, cough, dyspnea, pleural effusion, pneumothorax, interstitial pneumonia
SKIN: Alopecia, carcinoma, diaphoresis, ecchymosis, exfoliative dermatitis, pruritus, ulcer, vesiculobullous rash
Other: Angioedema, flu syndrome, hypersensitivity reaction, hypocalcemia, weight loss

Cautions

WARNING Notify prescriber immediately if patient has evidence of hypertensive crisis, such as blurred vision, chest pain, difficulty thinking, stupor or coma, seizures, severe headache, neck stiffness, nausea, vomiting, palpitations or signs and symptoms suggesting a stroke. Expect to stop drug immediately if these occur.

Keep phentolamine readily available to treat hypertensive crisis. Give 5 mg by slow I.V. infusion, as prescribed, to reduce blood pressure without causing excessive hypotension. Use external cooling measures, as prescribed, to manage fever.

Monitor patient receiving rasagline with levodopa for worsening of pre-existing dyskinesia. If it occurs, notify prescriber and expect levodopa dosage to be decreased.

PATIENT SAFTY

WARNING Inform patient taking recommended dosage of rasagline that dietary tyramine restriction is no longer needed except for avoidance of very tyramine-rich such as aged cheese (e.g., Stilton), which may increase blood pressure greatly. If patient doesn’t feel well soon after eating a suspected high-tyramine meal, he should contact prescriber immediately.

Advise patient to stop taking rasagline and to notify prescriber immediately if he develops blurred vision, chest pain, trouble thinking, stupor or coma, seizures, severe headache, stiff neck, nausea, vomiting, palpitations, or evidence of stroke.

Suggest that patient change position slowly to minimize orthostatic hypotension.

Alert patient that drug may cause hallucinations. If they occur, tell patient to notify prescriber promptly.

Instruct patient to notify all prescribers of rasagline therapy, especially if antidepressants or antibiotics such as ciprofloxacin or a similar drug are being considered, and to avoid taking any over the counter cold medications.

Category

Chemical class: Tetrameric protein
Therapeutic class: Uric acid reducer

Pregnancy category: C

Indications

To manage plasma uric acid levels initially in patients with leukemia, lymphoma, or solid tumor malignancies who receive anticancer therapy that elevates plasma uric acid
IV: Adults and children. 0.20 mg/kg infused over 30 min daily for 5 days.

Mechanism of Action

Converts uric acid into an inactive and soluble metabolite at the end of the purine catabolic pathway. This prevents plasma uric acid levels from rising due to tumor lysis from anticancer therapy.

Contraindications

Glucose-6-phosphatase dehydrogenase (G6PD) deficiency; history of anaphylaxis or hypersensitivity reactions, hemolytic reactions, or methemoglobinemia reactions; hypersensitivity to rasburicase or its components

Side Efect

CNS: Anxiety, fever, headache, paresthesia, rigors, seizures
CV: Arrhythmia, cardiac failure or arrest, cerebrovascular disorder, chest pain, hemorrhage, hypotension, myocardial infarction, pulmonary edema, thrombophlebitis, thrombosis
EENT: Mucositis, retinal hemorrhage
ENDO: Hot flashes
GI: Abdominal pain, constipation, diarrhea, ileus, intestinal obstruction, nausea, vomiting
GU: Acute renal failure
HEME: Anemia, hemolysis, methemoglobinemia, neutropenia, pancytopenia
RESP: Cyanosis, dyspnea, pneumonia, pulmonary hypertension, respiratory distress
SKIN: Cellulitis, rash
Other: Anaphylaxis, dehydration, infection, sepsis

Cautions

Be aware that children at high risk for G6PD deficiency, such as patients of African or Mediterranean ancestry, should be screened before administering rasburicase because severe hemolysis can occur.

Expect to give only one course of therapy because of risk of severe allergic reactions.

Reconstitute rasburicase using only diluent provided. Add 1 ml of diluent to each vial needed, and mix by swirling very gently. Don’t shake or invert vial.

Inject reconstituted solution into an infusion bag containing the appropriate volume of normal saline solution to obtain a final volume of 50 ml. Infuse over 30 minutes in a different line than for infusion of other . If a separate line isn’t possible, flush the line with at least 15 ml of normal saline solution before and after rasburicase infusion. Don’t use filters.

Store reconstituted solution at 2° to 8° C (36° to 46° F) for no longer than 24 hours. Protect drug from light.
WARNING Monitor patient closely for severe hypersensitivity reactions, including anaphylaxis (chest pain, dyspnea, hypotension, urticaria), hemolysis (severe anxiety, pain, dyspnea), and methemoglobinemia (anxiety, hypoxemia, shortness of breath). If such a reaction occurs, discontinue rasburicase immediately, notify prescriber, and start emergency treatment. Rasburicase shouldn’t be restarted after such a reaction occurs.

Ensure that blood samples to measure uric acid levels are collected in chilled tubes containing heparin anticoagulant and are immediately placed in ice water until analysis is done (within 4 hours); blood samples left at room temperature will result in low uric acid levels because of enzyme degradation of uric acid at room temperature.

PATIENT SAFTY

Explain to child and parents that chemotherapy will start 4 to 24 hours after rasburicase.

Stress the importance of reporting any adverse reaction immediately.

Category

Chemical class: Fentanyl analogue
Therapeutic class: Anesthesia adjunct

Pregnancy category: C

Controlled substance schedule: II

Indications

As adjunct to induce general anesthesia INTERMITTENT
IV: Adults and children age 2 and over. 0.5 to 1 mcg/kg plus inhalation or I.V. anesthetic. To maintain general anesthesia INTERMITTENT
IV: Adults and children age 2 and over. 0.05 to 0.2 mcg/kg, followed by 0.5 to 1 mcg/kg every 2 to 5 min, as needed. To continue analgesic effect in immediate postoperative period CONTINUOUS
IV: Adults and children age 2 and over.Initial: 0.1 mcg/kg/min, adjusted by 0.025 mcg/kg/ min every 5 min, as prescribed, to balance level of analgesia and respiratory rate. Maximum: 0.2 mcg/kg/min. To supplement local or regional anesthesia in a monitored anesthetic setting
IV: Adults and children age 2 and over.With a benzodiazepine: 0.05 mcg/kg/min, starting 5 min before placement of local or regional block; after placement of block, decreased to 0.025 mcg/kg/min and then further adjusted every 5 min in increments of 0.025 mcg/kg/min, as needed. Without a benzodiazepine: 0.1 mcg/kg/min, starting 5 min before placement of local or regional block; after placement of block, decreased to 0.05 mcg/kg/min and then further adjusted every 5 min in increments of 0.025 mcg/kg/min, as needed.
I.V.INJECTION Adults and children age 2 and over. With a benzodiazepine: 0.5 mcg/kg over 30 to 60 sec as a single dose 60 to 90 sec before local anesthetic is administered. Without a benzodiazepine: 1 mcg/kg administered over 30 to 60 sec as a single dose 60 to 90 sec before local anesthetic is administered.
DOSAGE ADJUSTMENT For elderly patients, starting dose possibly reduced by half. If patient is more than 30% over ideal body weight, starting dose based on ideal body weight. Route Onset Peak Duration I.V. 1 min 1–2 min 5–10 min

Incompatibilities

Don’t give remifentanil through same I.V. line as blood because nonspecific esterases in blood products may inactivate drug.

Contraindications

Epidural or intrathecal administration, hypersensitivity to fentanyl analogues

Interactions

anesthetics (barbiturate, inhalation), benzoremifentanil hydrochloride 902 diazepines, propofol: Possibly synergistic effects, increasing risk of hypotension and respiratory depression atropine, glycopyrrolate: Possibly reversal of remifentanil-induced bradycardia ephedrine, epinephrine, norepinephrine: Possibly reversal of remifentanil-induced hypotension neuromuscular blockers: Prolonged skeletal muscle rigidity caused by remifentanil opioid antagonists: Possibly reversal of remifentanil’s effects

Side Efect

CNS: Headache, shivering
CV: Asystole, bradycardia, hypotension
GI: Nausea, vomiting
MS: Skeletal muscle rigidity
RESP: Apnea, cough, dyspnea, respiratory depression, stridor, wheezing
Other: Anaphylaxis

Cautions

Inject remifentanil into I.V. tubing at or as close as possible to venous cannula.

Use infusion device to deliver continuous infusion.

Monitor vital signs and oxygenation continuously during administration.

Expect analgesic effects to dissipate rapidly when drug is discontinued. Expect to start adequate postoperative analgesia, as prescribed, before stopping drug.
WARNING After stopping drug, clear I.V. tubing to prevent inadvertent later delivery.

Monitor respiratory status continuously because of risk of respiratory depression from residual effects of other anesthetics for up to 30 minutes after infusion stops.

PATIENT SAFTY

Explain expected drug effects to patient, and reassure her that she’ll be monitored continuously during drug administration.

Category

Chemical class: Meglitinide
Therapeutic class: Antidiabetic

Pregnancy category: C

Indications

To achieve glucose control in type 2 diabetes mellitus as monotherapy in patients whose glycosylated hemoglobin (HbA1c) level is less than 8%
Adults. Initial: 0.5 mg 15 to 30 min before meals b.i.d. Dosage doubled, as needed, every wk until adequate glucose response obtained. Maintenance: 0.5 to 4 mg/dose up to q.i.d. Maximum: 16 mg daily in divided doses of not more than 4 mg/dose. To achieve glucose control in type 2 diabetes mellitus as monotherapy in patients whose HbA1cis 8% or greater and in combination with metformin or thiazolidinedione (pioglitazone Adenyl cyclase K+ cAMP Ca++ Remifentanil Neuron Substance P Mu-opioid receptor

Mechanism of Action

Remifentanil decreases transmission and perception of pain by stimulating mu-opioid receptors in neurons. This action decreases the activity of adenyl cyclase in neurons, which in turn decreases cAMP production. With less cAMP available, potassium (K+) is forced out of neurons, and calcium (Ca++) is prevented from entering neurons. As a result, neuron excitability declines, and fewer neurotransmitters (such as substance P) leave the neurons, thereby decreasing pain transmission. hydrochloride, rosiglitazone maleate) therapy
Adults. Initial: 1 or 2 mg 15 to 30 min before meals b.i.d. Dosage doubled, as needed, every wk until adequate glucose response obtained. Maintenance: 1 to 4 mg/ dose up to q.i.d. Maximum: 16 mg daily in divided doses of not more than 4 mg/dose.
DOSAGE ADJUSTMENT For patients with moderate to severe hepatic or renal impairment, increased time between dosage adjustments.

Mechanism of Action

Stimulates release of insulin from functioning pancreatic beta cells. In patients with type 2 diabetes mellitus, a shortage of these cells decreases blood insulin levels and causes glucose intolerance. By interacting with the adenosine triphosphatase (ATP)–potassium channel on the beta cell membrane, repaglinide prevents potassium from leaving the cell. This causes the beta cell to depolarize and the cell membrane’s calcium channel to open. As a result, calcium moves into the cell and insulin moves out. The extent of insulin release is glucose dependent; the lower the glucose level, the less insulin is secreted from the cell.

Contraindications

Concurrent therapy with gemfibrozil, diabetic ketoacidosis, hypersensitivity to repaglinide or its components, severe hepatic or renal impairment, type 1 diabetes mellitus

Interactions

barbiturates, carbamazepine, rifampin, troglitazone: Possibly increased repaglinide metabolism beta blockers, chloramphenicol, clarithromycin, MAO inhibitors, NSAIDs, oral anticoagulants, probenecid, salicylates, sulfonamides: Enhanced hypoglycemic effects calcium channel blockers, corticosteroids, diuretics, estrogens, isoniazid, niacin, oral contraceptives, phenothiazines, phenytoin, sympathomimetics, thyroid hormones: Possibly loss of glucose control erythromycin, ketoconazole, miconazole: Possibly inhibited repaglinide metabolism gemfibrozil: Increased blood repaglinide level, resulting in enhanced and prolonged blood glucose–lowering effects NPH insulin: Possibly increased risk of angina OATP1B1 inhibitors such as cyclosporine, trimethoprim: Increased plasma repaglinide level

Side Efect

CNS: Headache
CV: Angina
EENT: Rhinitis, sinusitis
ENDO: Hypoglycemia
GI: Diarrhea, elevated liver enzymes, hepatitis, nausea, pancreatitis
HEME: Hemolytic anemia, leukopenia, thrombocytopenia
MS: Arthralgia, back pain
RESP: Bronchitis, upper respiratory tract infection
SKIN: Alopecia, Stevens-Johnson syndrome
Other: Anaphylaxis

Cautions

Be aware that repaglinide shouldn’t be used with NPH insulin because the combination may increase the risk of angina.

Expect to check HbA1clevel every 3 months, as ordered, to assess patient’s long-term control of blood glucose level.

During times of increased stress, such as from infection, surgery, or trauma, monitor blood glucose level often and assess need for additional insulin.

PATIENT SAFTY

Instruct patient to take repaglinide 15 to 30 minutes before meals and to skip dose whenever she skips a meal.

Explain that repaglinide is an adjunct to diet in managing type 2 diabetes mellitus.

Inform patient that changes in blood glucose level may cause blurred vision or visual disturbances, especially when repaglinide therapy starts. Reassure him that these changes are usually transient.

Teach patient how to monitor her blood glucose level and when to notify prescriber about changes.

Review signs and symptoms of hyperglycemia and hypoglycemia with patient and family. Instruct patient to notify prescriber immediately if she experiences anxiety, confusion, dizziness, excessive sweating, headache, increased thirst, increased urination, or nausea.

Advise patient to wear or carry identification indicating that she has diabetes. Encourage her to carry candy or other simple carbohydrates with her to treat mild episodes of hypoglycemia.

Inform patient that her HbA1clevel will be tested every 3 to 6 months until her blood glucose level is controlled.

Category

Chemical class: Rauwolfia alkaloid
Therapeutic class: Antihypertensive

Pregnancy category: C

Indications

To treat hypertension
Adults. 0.1 to 0.25 mg daily. Children. 0.005 to 0.02 mg/kg daily once daily or in divided doses b.i.d.
DOSAGE ADJUSTMENT Lower dosage possibly required for elderly or severely debilitated patients. Route Onset Peak Duration P.O. Days–3 wk 3–6 wk 1–6 wk

Contraindications

Active peptic ulcer, electroconvulsive therapy, hypersensitivity to reserpine or its components, mental depression (current or history of), ulcerative colitis

Interactions

anticholinergics: Decreased effectiveness of anticholinergics barbiturates: Increased CNS depression
beta blockers: Additive and, possibly, excessive beta-adrenergic blockade bromocriptine: Possibly interference with Norepinephrine Vesicle Sympathetic neuron Norepinephrine reuptake Beta receptor Cell membrane Alpha receptor Reserpine displaces norepinephrine MAO degrades norepinephrine Norepinephrine Vesicle Sympathetic neuron Norepinephrine reuptake Beta receptor Cell membrane Alpha receptor Reserpine displaces norepinephrine MAO degrades norepinephrine

Mechanism of Action

Reserpine reduces blood pressure by decreasing norepinephrine stores in presynaptic sympathetic neurons. Normally, when a nerve impulse activates a sympathetic neuron, the nerve ending releases norepinephrine, which stimulates alpha or beta receptors on target cell membranes, as shown below left. Stimulation of alpha receptors may produce vasoconstriction; stimulation of beta receptors may increase heart rate and force of myocardial contraction, which raises cardiac output. Through a reuptake mechanism, some norepinephrine returns to the neuron and is stored in vesicles for reuse. Reserpine displaces norepinephrine from vesicles in the nerve fiber, and MAO degrades the displaced norepinephrine, as shown below right. These actions reduce the amount of norepinephrine available to stimulate postsynaptic alpha and beta receptors, reducting vasoconstriction, cardiac output, and blood pressure. bromocriptine’s effects digoxin, procainamide,
quinidine: Increased risk of arrhythmias hypotension-producing : Increased antihypertensive effect; increased risk of orthostatic hypotension or bradycardia (with guanadrel or guanethidine) levodopa: Decreased levodopa effectiveness
MAO inhibitors: Increased risk of severe hypertension and hyperpyrexia, additive CNS depression
NSAIDs: Decreased antihypertensive effect sympathomimetics: Increased vasopressor effects, decreased antihypertensive effect
alcohol use: Increased CNS depression

Side Efect

CNS: Anxiety, depression, dizziness, drowsiness, headache, nervousness, nightmares, sleep disturbance, syncope, weakness
CV: Arrhythmias, such as bradycardia; chest pain; peripheral edema
EENT: Conjunctival injection, dry mouth, epistaxis, glaucoma, hearing loss, nasal congestion, optic atrophy, uveitis
ENDO: Breast engorgement
GI: Abdominal cramps or pain, anorexia, diarrhea, increased gastric secretions, melena, nausea, vomiting
GU: Decreased libido, galactorrhea, gynecomastia, impotence
MS: Myalgia
RESP: Dyspnea
SKIN: Purpura
Other: Weight gain

Cautions

If patient has a history of depression, use reserpine cautiously because it may cause depression masked as somatic complaints.

Monitor blood pressure frequently during drug therapy.

Alert anesthesiologist if patient is scheduled for surgery. Drug may cause circulatory instability even if withheld before procedure.

PATIENT SAFTY

Instruct patient to take reserpine with food or milk to minimize stomach upset.

Caution patient about possible drowsiness, and advise her to avoid potentially hazardous activities until drug’s CNS effects are known.

Explain the need for frequent appointments to monitor blood pressure and adjust dosage at start of therapy.

Category

Chemical class: Recombinant plasminogen activator (r-PA)
Therapeutic class: Thrombolytic

Pregnancy category: C

Indications

To improve ventricular function, prevent heart failure, and reduce mortality after acute MI
I.V.INJECTION
Adults. 10 units over 2 min; repeated after 30 min.

Mechanism of Action

Converts plasminogen to plasmin, which works to break up fibrin clots that have formed in the coronary arteries. Elimination of the clots improves cardiac blood and oxygen flow to the area, thus improving ventricular function.

Incompatibilities

Don’t add other to reteplase injection solution or administer them through same I.V. line as reteplase.

Contraindications

Active internal bleeding, aneurysm, arteriovenous malformation, bleeding diathesis, brain tumor, history of stroke or other cerebrovascular disease, hypersensitivity to reteplase or its components, intracranial or intraspinal surgery or trauma during previous 2 months, severe uncontrolled hypertension (systolic 200 mm Hg or higher, diastolic 110 mm Hg or higher)

Interactions

antifibrinolytics (including aminocaproic acid, aprotinin, and tranexamic acid): Decreased effectiveness of reteplase antineoplastics, antithymocyte globulin, certain cephalosporins (such as cefamandole, cefoperazone, and cefotetan), heparin, oral anticoagulants, platelet aggregation inhibitors (such as abciximab, aspirin, and dipyridamole), strontium-89 chloride, sulfinpyrazone,
valproic acid: Increased risk of bleeding

Side Efect

CNS: Intracranial hemorrhage
GI: GI bleeding, nausea, vomiting
HEME: Thrombocytopenia
RESP: Hemoptysis
SKIN: Bleeding from wounds, ecchymosis, hematoma, purpura
Other: Allergic reaction, injection site bleeding

Cautions

Expect to start reteplase, as prescribed, as soon as possible after MI symptoms begin.

Closely monitor patient with atrial fibrillation, severe hypertension, or other cardiac disease for signs and symptoms of cerebral embolism.

To reconstitute, use diluent, syringe, needle, and dispensing pin provided. Withdraw 10 ml of preservative-free sterile water for injection. Remove and discard needle from syringe, and connect dispensing pin to syringe. Remove protective cap from spike end of dispensing pin, and insert spike into reteplase vial. Inject 10 ml of sterile water into the vial. With the spike still in the vial, swirl gently to dissolve the powder. Don’t shake. Expect to see slight foaming. Let the vial stand for several minutes. When the bubbles dissipate, withdraw 10 ml of reconstituted solution into the syringe (about 0.7 ml may remain in the vial). Now detach the syringe from the dispensing pin and attach the 20G needle.

Use the solution within 4 hours. Discard if it’s discolored or contains particulates.

Don’t give heparin and reteplase in the same solution. Instead, flush the heparin line with normal saline solution or D5W before and after reteplase injection.

Because fibrin is lysed during therapy, closely monitor all possible bleeding sites (catheter insertions, arterial and venous punctures, cutdowns, and needle punctures).

Avoid I.M. injections, venipunctures, and nonessential handling of patient during therapy.

If arterial puncture is needed, use an arm vessel that can be compressed, if possible. After sample is obtained, apply pressure for at least 30 minutes; then apply a pressure dressing. Check site often for bleeding.

If bleeding occurs and can’t be controlled by local pressure, notify prescriber immediately. Be prepared to stop anticoagulant therapy immediately and to discontinue second reteplase bolus, as prescribed.

Anticipate that reperfusion arrhythmias, such as premature ventricular contractions or ventricular tachycardia, may follow coronary thrombolysis.

PATIENT SAFTY

Advise patient to report

Side Efect

immediately.

Category

Chemical class: Spiropiperidyl derivative
Therapeutic class: Antimycobacterial antibiotic

Pregnancy category: B

Indications

To prevent disseminated Mycobacterium avium complex in patients with advanced HIV infection
Adults. 300 mg once daily or 150 mg b.i.d.

Mechanism of Action

Suppresses RNA synthesis by inhibiting DNA-dependent RNA polymerase in a wide variety of bacteria, including Mycobacterium avium. Exhibits dose-dependent bactericidal or bacteriostatic action.

Contraindications

Hypersensitivity to rifabutin or rifamycins

Interactions

aminophylline, barbiturates, beta blockers, chloramphenicol, clofibrate, corticosteroids, cyclosporine, dapsone, diazepam, digoxin, disopyramide, estramustine, estrogens, ketoconazole, mexiletine, oral anticoagulants, oral antidiabetic , oral contraceptives (containing estrogen), oxtriphylline, phenytoin, quinidine, theophylline, tocainide, verapamil (oral): Reduced effects of these fluconazole: Increased blood rifabutin level methadone: Possibly withdrawal symptoms zidovudine: Decreased blood zidovudine level

Side Efect

CNS: Asthenia, fever, headache, insomnia
CV: Chest pain
EENT: Discolored saliva, tears, and sputum
GI: Abdominal pain, anorexia, diarrhea, discolored feces, elevated liver function test results, eructation, flatulence, indigestion, nausea, pseudomembranous colitis, vomiting
GU: Discolored urine
HEME: Neutropenia, thrombocytopenia
MS: Myalgia
SKIN: Discolored skin and sweat, rash

Cautions

Monitor laboratory values during rifabutin therapy to detect neutropenia and thrombocytopenia.

Expect drug to cause reddish orange to reddish brown discoloration of skin and body fluids.

Be aware that drug may cause myelosuppression and increased risk of infection. Notify prescriber immediately if signs of infection, such as fever, develop.

Monitor patient for diarrhea during therapy and for at least 2 months afterward; diarrhea may signal pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold rifabutin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

PATIENT SAFTY

Advise patient to take rifabutin with food if GI distress develops.

Encourage patient to have needed dental work done before rifabutin therapy starts to reduce the risk of bleeding or infection.

Explain that drug may turn urine, feces, saliva, sputum, sweat, tears, and skin reddish orange to reddish brown.

Caution patient against wearing soft contact lenses during therapy because drug may permanently stain them.

Advise patient to notify prescriber about signs of Mycobacterium avium complex (chills, fever, night sweats, weight loss), tuberculosis, myositis, or uveitis.

Advise woman of childbearing age that rifabutin may decrease effectiveness of oral contraceptives; advise her to use a nonhormonal method of birth control.

Urge patient to tell prescriber about diarrhea that’s severe or prolonged. Remind patient that watery or bloody stools can occur 2 months or more after antibiotic therapy ends and can be serious, requiring prompt treatment.

Category

Chemical class: Semisynthetic antibiotic derivative of rifamycin
Therapeutic class: Antimycobacterial antitubercular

Pregnancy category: C

Indications

As adjunct to treat tuberculosis caused by all strains of Mycobacterium tuberculosis , ORAL SUSPENSION,
IV:
Adults. 10 mg/kg daily with other antitubercular for 2 mo. Maximum: 600 mg daily. Infants and children.10 to 20 mg/kg daily in combination with other antitubercular for 2 mo. Maximum: 600 mg daily. To eliminate meningococci from nasopharynx of asymptomatic carriers of Neisseria meningitidis , ORAL SUSPENSION,
IV:
Adults. 600 mg every 12 hr for 2 days (total of 4 doses). Infants age 1 month and over and children. 10 mg/kg every 12 hr for 2 days (total of 4 doses). Maximum: 600 mg daily. Infants under age 1 month. 5 mg/kg every 12 hr for 2 days (total of 4 doses). Maximum: 600 mg daily.
DOSAGE ADJUSTMENT For patients with hepatic impairment, maximum of 8 mg/kg daily. For patients with creatinine clearance of 10 ml/min/1.73 m2or less, recommended dosage usually decreased by 50%.

Mechanism of Action

Inhibits bacterial and mycobacterial RNA synthesis by binding to DNA-dependent RNA polymerase, thereby blocking RNA transcription. Exhibits dose-dependent bactericidal or bacteriostatic action. Rifampin is highly effective against rapidly dividing bacilli in extracellular cavitary lesions, such as those found in the nasopharynx.

Incompatibilities

Don’t administer rifampin in the same I.V. line as diltiazem.

Contraindications

Concurrent use of nonnucleoside reverse transcriptase inhibitors or protease inhibitors by patients with HIV, hypersensitivity to rifamycins

Interactions

aminophylline, oxtriphylline,
theophylline: Increased metabolism and clearance of these theophylline preparations anesthetics (hydrocarbon inhalation, except isoflurane), hepatotoxic , isoniazid: Increased risk of hepatotoxicity beta blockers, chloramphenicol, clofibrate, corticosteroids, cyclosporine, dapsone, digitalis glycosides, disopyramide, hexobarbital, itraconazole, ketoconazole, mexiletine, oral anticoagulants, oral antidiabetic , phenytoin, propafenone, quinidine, tocainide, verapamil (oral): Increased metabolism, resulting in lower blood levels of these bone marrow depressants: Increased leukopenic or thrombocytopenic effects clofazimine: Reduced absorption of rifampin, delaying its peak concentration and increasing its half-life diazepam: Enhanced diazepam elimination, resulting in decreased drug effectiveness estramustine, estrogens, oral contraceptives: Decreased estrogenic effects methadone: Possibly impaired absorption of methadone, leading to withdrawal symptoms probenecid: Increased blood level or prolonged duration of rifampin, increasing risk of toxicity nonnucleoside reverse transcriptase inhibitors, protease inhibitors (indinavir, nelfinavir, ritonavir, saquinavir): Accelerated metabolism of these (by patients with HIV), resulting in subtherapeutic levels; delayed metabolism of rifampin, increasing risk of toxicity trimethoprim: Increased elimination and shortened elimination half-life of trimethoprim
vitamin D: Increased metabolism and decreased efficacy of vitamin D, leading to decreased serum calcium and phosphate levels and increased parathyroid hormone levels
alcohol use: Increased risk of hepatotoxicity

Side Efect

CNS: Chills, dizziness, drowsiness, fatigue, headache, paresthesia
EENT: Discolored saliva, tears, and sputum; mouth or tongue soreness; periorbital edema
GI: Abdominal cramps, anorexia, diarrhea, discolored feces, elevated liver function test results, epigastric discomfort, flatulence, heartburn, hepatitis, nausea, pseudomembranous colitis, vomiting
GU: Discolored urine
MS: Arthralgia, myalgia
SKIN: Discolored skin and sweat
Other: Facial edema, flulike symptoms

Cautions

Obtain blood samples or other specimens for culture and sensitivity testing, as ordered, before giving rifampin and throughout therapy to monitor response to drug.

Expect to monitor liver function test results before and every 2 to 4 weeks during therapy. Immediately report abnormalities.

For I.V. infusion, reconstitute by adding 10 ml sterile water for injection to 600-mg vial of rifampin. Swirl gently to dissolve. Withdraw appropriate dose and add to 500 ml D5W (preferred solution) or normal saline solution and infuse over 3 hours. Or, withdraw appropriate dose and add to 100 ml D5W (preferred solution) or normal saline solution and infuse over 30 minutes. Use reconstituted drug promptly because rifampin may precipitate out of D5W solution after 4 hours. In normal saline solution, drug is stable up to 24 hours at room temperature.

Be aware that patient receiving intermittent therapy (once or twice weekly) is at increased risk for

Side Efect

.

Expect drug to discolor skin and body fluids reddish orange to reddish brown.

Be aware that rifampin can cause myelosuppression and increase risk of infection. Notify prescriber immediately if signs of infection, such as fever, develop.

PATIENT SAFTY

Instruct patient to take rifampin 1 hour before or 2 hours after a meal with a full glass of water.

Stress the need to take drug exactly as prescribed. Explain that interruptions can lead to increased

Side Efect

.

Explain that drug may turn urine, feces, saliva, sputum, sweat, tears, and skin reddish orange to reddish brown.

Caution patient against wearing soft contact lenses during therapy because drug may permanently stain them.

Advise patient who takes an oral contraceptive to use an additional form of birth control during rifampin therapy.

Urge patient to notify prescriber about flulike symptoms, anorexia, darkened urine, fever, joint pain or swelling, malaise, nausea, vomiting, and yellowish skin or eyes, which may indicate hepatitis.

Advise patient to avoid alcohol during rifampin therapy.

Instruct patient to notify prescriber if no improvement occurs within 2 to 3 weeks.

Category

Chemical class: Benzothiazole
Therapeutic class: Amyotrophic lateral sclerosis treatment agent

Pregnancy category: C

Indications

To treat amyotrophic lateral sclerosis
Adults. 50 mg every 12 hr.

Mechanism of Action

Inhibits release of glutamic acid, an excitatory amino acid neurotransmitter, in the CNS, thus reducing its effects on target cells. Glutamic acid affects degeneration of neurons; reducing its level may help slow amyotrophic lateral sclerosis.

Contraindications

Hypersensitivity to riluzole or its components

Interactions

allopurinol, hepatotoxic , methyldopa, sulfasalazine: Increased risk of hepatotoxicity amitriptyline, phenacetin, quinolones, tacrine,
theophylline: Delayed elimination of riluzole omeprazole,
rifampin: Increased riluzole clearance charbroiled : Increased riluzole elimination
alcohol use: Increased risk of hepatotoxicity smoking: Increased riluzole elimination

Side Efect

CNS: Asthenia, dizziness, headache, insomnia, paresthesia (circumoral), somnolence, spasticity, vertigo
CV: Peripheral edema
EENT: Dry mouth, rhinitis, stomatitis
GI: Abdominal pain, anorexia, constipation, diarrhea, elevated liver function test results, flatulence, hepatitis, indigestion, nausea, vomiting
HEME: Neutropenia
MS: Back or muscle pain or stiffness
RESP: Dyspnea, hypersensitivity pneumonitis, increased cough, interstitial lung disorder, pneumonia
SKIN: Alopecia, eczema, pruritus
Other: Anaphylaxis

Cautions

Use riluzole cautiously in patients with impaired hepatic or renal function.

Also use cautiously in elderly patients, women, and Japanese patients because of increased risk of toxicity from decreased drug clearance.

Monitor liver function test results before and during riluzole therapy.

Monitor patient for respiratory symptoms, such as dry cough or dyspnea. Notify prescriber if present, and expect patient to have a chest X-ray, as ordered. If evidence of interstitial lung disease or hypersensitivity pneumonitis is present, expect riluriluzole 910 zole to be discontinued immediately.

PATIENT SAFTY

Instruct patient to take riluzole regularly, every 12 hours, either 1 hour before or 2 hours after a meal, and at the same time each day.

Instruct patient to store riluzole at room temperature, protected from bright light.

Urge patient to minimize alcohol, smoking, and charred because they speed drug excretion.

Tell patient to report fever, cough, or difficulty breathing.

Category

Chemical class: Pyridinyl bisphosphonate
Therapeutic class: Bone resorption inhibitor

Pregnancy category: C

Indications

To treat Paget’s disease of bone when serum alkaline phosphatase level is at least twice normal and patient is symptomatic or at risk for complications
Adults. 30 mg daily for 2 mo. Repeated after 2 mo if relapse occurs or if serum alkaline phosphatase level fails to normalize. To prevent or treat glucocorticoidinduced osteoporosis
Adults. 5 mg daily. Or, for postmenopausal osteoporosis, 35 mg once/wk or 75 mg taken on 2 consecutive days once/mo. To prevent or treat postmenopausal osteoporosis
Adults. 5 mg daily. Or, 35 mg once weekly, 75 mg taken on 2 consecutive days once a month, or 150 mg once a month To treat osteoporosis in men
Adults. 35 mg once/wk. Route Onset Peak Duration P.O. Unknown 3 mo 16 mo

Mechanism of Action

Hinders excessive bone remodeling characteristic of Paget’s disease by binding to bone and reducing the rate at which osteoclasts are resorbed by bone.

Contraindications

Esophageal abnormalities that delay esophageal emptying, such as stricture or achalasia; hypersensitivity to risedronate or its components; inability to stand or sit upright for at least 30 minutes; hypocalcemia

Interactions

aspirin,
NSAIDs: Increased risk of GI irritation calcium-containing preparations, including antacids: Impaired absorption of risedronate all : Decreased risedronate bioavailability

Side Efect

CNS: Anxiety, asthenia, depression, dizziness, fatigue, headache, insomnia, sciatica, syncope, vertigo, weakness
CV: Chest pain, hypercholesterolemia, hypertension, peripheral edema, vasodilation
EENT: Amblyopia, cataract, dry eyes, nasopharyngitis, pharyngitis, rhinitis, sinusitis, tinnitus
GI: Abdominal pain, colitis, constipation, diarrhea, dyspepsia, dysphagia, eructation, esophagitis, esophageal or gastric ulcers, flatulence, gastritis, nausea, vomiting
GU: UTI
MS: Arthralgia; back, limb, neck, or shoulder pain; jaw osteonecrosis; leg cramps or spasms; myasthenia; myalgia; osteoarthritis
RESP: Bronchitis, cough, pneumonia, upper respiratory tract infection
SKIN: Bullous reaction, pruritus, rash
Other: Angioedema, flulike symptoms, hypersensitivity reaction, hypocalcemia

Cautions

Risedroante isn’t recommended for patients with severe renal impairment.

Make sure patient has had a dental checkup before having invasive dental procedures during risedroante therapy, especially if patient has cancer; is receiving chemotherapy, head or neck radiation, or a corticosteroid; or has poor oral hygiene because risk of osteonecrosis is increased in these patients.

Give supplemental calcium and vitamin D, as prescribed, during risedronate therapy if patient’s dietary intake is inadequate.

Give calcium supplements and antacids at different time of day than risedronate administration to avoid impaired drug absorption and altered effectiveness.

Watch for rare but possibly severe rash, bullous skin reactions, and angioedema.

PATIENT SAFTY

Instruct patient to take risedronate at least 1 hour before first food or drink of day (except water) while in an upright position and with 6 to 8 oz of water. Caution against lying down for at least 30 minutes after taking drug to keep it from lodging in esophagus and causing irritation. Also instruct patient not to chew or suck on tablet because doing so may irritate mouth or throat.

Advise patient to stop taking risedronate and to notify prescriber if GI symptoms appear or become worse.

Alert patient that in the same class as risedronate have caused severe bone, joint, or muscle pain. If such symptoms appear while taking risedronate, advise patient to contact prescriber.

If patient takes 35 mg once weekly and misses a dose, tell her to take it the morning after she remembers and then to take the next dose on its usual day. If patient takes 75 mg on 2 consecutive days once monthly and she misses both doses with more than 7 days until the next scheduled dose, tell her to take the first missed dose on the morning after she remembers and the second dose the following day. If she misses only one of the two doses, tell her to take it the morning after she remembers and then resume her normal schedule. If patient takes 150 mg once monthly and misses a dose, urge her to contact prescriber for instructions. Caution patient not to take more than 150 mg within a 7day period and not to take two tablets of any strength on the same day.

Tell patient to take calcium supplements or antacids at different times than risedronate.

Urge women of childbearing age to tell prescriber about planned, suspected, or known pregnancy because of risk to fetal skeleton.

Tell patient to stop risedronate and contact prescriber about swelling or skin abnormalities.

Instruct patient on proper oral hygiene and on the need to notify prescriber about invasive dental procedures.

Category

Chemical class: Benzisoxazole derivative
Therapeutic class: Antipsychotic

Pregnancy category: C

Indications

To manage psychotic disorders

ORALL

, ORALLY DISINTEGRATING ,
Adults. 1 mg b.i.d. on day 1; 2 mg b.i.d. on day 2; 3 mg b.i.d. on day 3. Or, 2 mg daily on day one; 4 mg daily on day two; 6 mg daily on day 3. Then increased by 1 to 2 mg daily at 1to 2-wk intervals, as needed. Maximum: 16 mg daily. Adolescents ages 13 to 17. Initial: 0.5 mg once daily, increased as needed every 24 hr in 0.5to 1-mg increments. Maximum: 3 mg once daily.
I.M.INJECTION(RISPERDAL CONSTA)
Adults. Initial: 25 mg every 2 wk, increased as needed every 4 wk to 37.5 or 50 mg. Maximum: 50 mg every 2 wk. To treat bipolar mania

ORALL

, ORALLY DISINTEGRATING ,
Adults. Initial: 2 or 3 mg daily, increased as needed by 1 mg daily up to 6 mg. Maximum: 6 mg daily for no more than 3 wk. Children and adolescents ages 10 to 17. Initial: 0.5 mg once daily, increased as needed every 24 hr in 0.5to 1-mg increments. Maximum: 2.5 mg once daily. To treat bipolar mania as monotherapy or as adjunct to lithium or valproate therapy
I.M.INJECTION(RISPERDAL CONSTA)
Adults. 25 mg every 2 wk., increased, as needed to 37.5 mg or 50 mg. Maximum: 50 mg every 2 wk.
DOSAGE ADJUSTMENT Initially 0.5 mg b.i.d. for elderly or debilitated patients, those with renal or hepatic impairment, and those at risk for hypotension. Increased by 0.5 mg b.i.d. every wk, as needed. Given daily after target dosage maintained for 2 or 3 days. Maximum for patients with severe hepatic dysfunction, 4 mg daily; for elderly patients, 3 mg daily. Initially 12.5 mg for patients receiving drug I.M. who have renal or hepatic impairment, take other that increase risperidone blood level, or have a history of tolerating psychotropic poorly. For adolescents and children with persistent somnolence, dose may be split and given twice daily. To treat irritability associated with autistic disorder

ORALL

, ORALLY DISINTEGRATING , Children age 5 and over and adolescents weighing less than 20 kg (44 lb). Initial: 0.25 mg daily, increased after 4 days to 0.5 mg daily. Dosage further increased, as needed in 2 wk intervals in 0.25 mg increments. Children age 5 and over and adolescents weighing 20 kg or more.Initial: 0.5 mg daily, increased after 4 days to 1 mg daily. Dosage further increased, as needed in 2 wk intervals in 0.5 mg increments.

Mechanism of Action

Selectively blocks serotonin and dopamine receptors in the mesocortical tract of the CNS to suppress psychotic symptoms.

Incompatibilities

Don’t mix oral solution with cola or tea.

Contraindications

Hypersensitivity to risperidone or its components

Interactions

antihypertensives: Increased antihypertensive effects bromocriptine, levodopa, pergolide: Possibly antagonized effects of these carbamazepine: Increased risperidone clearance with long-term concurrent use clozapine: Decreased risperidone clearance with long-term concurrent use
CNS depressants: Additive CNS depression fluoxetine, paroxetine: Increased plasma risperidone level
alcohol use: Additive CNS depression

Side Efect

CNS: Aggressiveness, agitation, akathisia, anxiety, asthenia, confusion, decreased concentration, dizziness, dream disturbances, drowsiness, dyskinesia, dystonia, fatigue, fever, headache, lassitude, memory loss, nervousness, neuroleptic malignant syndrome, parkinsonism, restlessness, seizures, somnolence, tremor
CV: Atrial fibrillation, chest pain, hypercholesterolemia, orthostatic hypotension, palpitations, QT-interval prolongation, tachycardia
EENT: Decreased or increased salivation, dry mouth, pharyngitis, retinal artery occlusion, rhinitis, sinusitis, vision changes
ENDO: Diabetic ketoacidosis (patients with diabetes), elevated prolactin level, galactorrhea, hyperglycemia, pituitary adenoma
GI: Abdominal pain, anorexia, constipation, diarrhea, indigestion, intestinal obstruction, nausea, vomiting
GU: Amenorrhea, decreased libido, dysmenorrhea, dysuria, hypermenorrhea, incontinence, increased appetite, polyuria, sexual dysfunction, UTI
HEME: Agranulocytosis, leukopenia, neutropenia
MS: Arthralgia, back pain, myalgia
RESP: Cough, dyspnea, sleep apnea, upper respiratory tract infection
SKIN: Diaphoresis, dry skin, hyperpigmentation, photosensitivity, pruritus, rash, seborrhea
Other: Anaphylaxis, angioedema, injection site induration, pain, redness, or swelling; weight gain or loss

Cautions

Use risperidone cautiously in debilitated patients, elderly patients, and patients with hepatic or renal dysfunction or hypotension because of their increased sensitivity to drug. Also use risperidone cautiously in patients with a history of seizures; although rare, seizures may occur in those with schizophrenia.
WARNING Be aware that risperidone should not be used to treat elderly patients with dementia-related psychosis because it increases risk of death in these patients.

Be aware that oral risperidone or another antipsychotic should be continued for 3 weeks after long-acting I.M. form of risperidone is first administered to provide an adequate therapeutic plasma level until risperidone release from injection site has begun. If the patient has never received oral risperidone, an oral trial should be prescribed before use of I.M. form to determine patient’s tolerance of the drug.

Remove I.M. form from refrigerator and allow it to come to room temperature before reconstitution. Follow manufacturer’s guidelines for reconstitution, using only the diluent supplied in the dose pack.

Give I.M. form using only the needle supplied in the dose pack. Inject entire contents of syringe into the upper outer quadrant of gluteal area within 2 minutes of reconstitution. If drug can’t be given right after reconstitution, shake the upright vial vigorously back and forth until particles are resuspended. Discard reconstituted drug if not used within 6 hours. Never administer I.M. form intravenously.

Monitor for orthostatic hypotension, especially in patients with cardiac or cerebrovascular disease.
WARNING Immediately notify prescriber and expect to stop giving risperidone if patient shows evidence of neuroleptic malignant syndrome (altered mental status, autonomic instability, hyperpyrexia, muscle rigidity), which can be fatal.

Monitor patient’s blood glucose and lipid levels as ordered because drug increases the risk of hyperglycemia and hypercholesterolemia.

Monitor patient’s CBC, as ordered, because serious adverse hematologic reactions may occur, such as agranulocytosis, leukopenia, or neutropenia. More frequent monitoring during the first few months of risperidone therapy is recommended for patients with a history of drug-induced leukopenia or neutropenia or who have had a significantly low WBC count in the past. If abnormalities occur during therapy, monitor patient for fever or other signs of infection, notify prescriber, and expect drug to be discontinued if severe.

PATIENT SAFTY

Instruct patient to dilute risperidone oral solution with water, coffee, orange juice, or low-fat milk but not with cola or tea.

Tell patient prescribed orally disintegrating tablets to break open the blister unit with dry hands by peeling the foil back to expose the tablet. Stress the importance of not pushing tablet through the foil because this could damage the tablet. Once patient has removed tablet, she should place immediately on her tongue, where it will dissolve within seconds. Tell patient not to chew orally disintegrating tablet or attempt to spit it out of her mouth.

Urge patient to avoid alcohol because of its additive CNS effects.

Caution diabetic patient to monitor blood glucose level closely because risperidone may increase it.

Category

Chemical class: Carbamate derivative
Therapeutic class: Antidementia

Pregnancy category: B

Indications

To treat mild to moderate Alzheimer’stype dementia ,
Adults. Initial: 1.5 mg b.i.d. Dosage increased by 3 mg daily every 2 wk, as needed. Maximum: 12 mg daily. TRANSDERMAL
Adults. Initial: 4.6 mg/24 hr. After 4 wk, increased to 9.5 mg/24 hr. To treat mild to moderate dementia in Parkinson’s disease ,
Adults. Initial: 1.5 mg b.i.d. Dosage increased by 3 mg daily every 4 wk, as needed. Maximum: 12 mg daily. TRANSDERMAL
Adults. Initial: 4.6 mg/24 hr. After 4 wk, increased to 9.5 mg/24 hr. To convert patient from oral to transdermal rivastigmine therapy TRANSDERMAL
Adults. If total oral dosage was less than 6 mg daily, use 4.6 mg/24 hr, with first transdermal patch applied the day after the last oral dose. If total oral dosage was 6 to 12 mg daily, use 9.5 mg/24 hr, with first transdermal patch applied the day after the last oral dose.
DOSAGE ADJUSTMENT If patient develops adverse effects (such as nausea or vomiting) during oral therapy, treatment should be stopped for several doses, as prescribed, restarted at lowest dose, and increased by 3 mg daily every 2 wk, as needed. If patient develops adverse effects during transdermal therapy, treatment should be discontinnued for several days and restarted at same or next lower dose level.

Mechanism of Action

May slow the decline of cognitive function in patients with Alzheimer’s disease by increasing acetylcholine concentration at cholinergic transmission sites. This action prolongs and exaggerates the effects of acetylcholine that are otherwise blocked by toxic levels of anticholinergics. The cognitive decline in these patients is partially related to cholinergic deficits along neuronal pathways projecting from the basal forebrain to the cerebral cortex and hippocampus that are involved in memory, attention, learning, and cognition.

Contraindications

Hypersensitivity to carbamate derivatives, rivastigmine, or their components

Interactions

anticholinergics: Possibly decreased effectiveness of anticholinergics bethanechol, succinylcholine: Possibly synergistic effects

Side Efect

CNS: Aggression, anxiety, asthenia, confusion, depression, dizziness, extrapyramidal movements, fatigue, fever, hallucinations, headache, insomnia, malaise, parkinsonism, seizures, somnolence, tremor
CV: Hypertension
EENT: Rhinitis
GI: Abdominal pain, anorexia, constipation, diarrhea, flatulence, indigestion, nausea, vomiting
GU: UTI
SKIN: Increased sweating, reaction at patch application site (pruritus, redness, swelling)
Other: Dehydration, flulike symptoms, weight loss

Cautions

WARNING Be aware that rivastigmine should be started at lowest recommended dosage and adjusted to effective maintenance dosage because initial therapy at high dosage can cause serious adverse GI reactions, including anorexia, nausea, and weight loss. Also, higher than recommended starting dosage may cause severe vomiting and possibly esophageal rupture. If treatment is interrupted for longer than several days, expect to restart at lowest recommended dosage.

Be aware that drug shouldn't be stopped abruptly because doing so may increase behavioral disturbances and precipitate a further decline in cognitive function.

Monitor respiratory status of patients with pulmonary disease, including asthma, chronic bronchitis, and emphysema, because rivastigmine has a weak affinity for peripheral cholinesterase, which may increase bronchoconstriction and bronchial secretions.

Monitor patient for adequate urine output because cholinomimetics, such as rivastigmine, may induce or exacerbate urinary tract or bladder obstruction.

Monitor patients with Parkinson’s disease for exaggerated parkinsonian symptoms, which may result from drug’s increased cholinergic effects on CNS.

PATIENT SAFTY

Explain to patient and family that rivastigmine can’t cure Alzheimer’s or Parkinson’s disease but may slow the progressive deterioration of memory and improve patient’s ability to perform activities of daily living.

Teach patient and family how to administer oral solution, if prescribed, emphasizing need to use the oral dosing syringe provided. Explain that dose may be swallowed directly from the syringe or mixed into a small glass of water, cold fruit juice, or soda; stirred; and then drunk.

Explain that oral drug should be taken with food to reduce adverse GI effects.

For transdermal patch, instruct patient or caregiver to apply it to clean, dry, hairless, intact skin in a location, such as the back, that won’t be rubbed by tight clothing and won’t be affected by lotion, cream, or powder. Tell patient to remove the old patch before applying a new one and to use a new application site daily. Caution against using the same site within 14 days.

To apply transdermal patch, tell patient to press patch firmly against skin until the edges stick well. Reassure patient that patch may be worn while swimming or bathing.

Instruct a family member to supervise patient’s use of rivastigmine.

Urge caregiver to contact prescriber and to withhold drug if patient stops taking it for more than several days.

Category

Chemical class: Selective 5-hydroxytryptamine
Therapeutic class: Antimigraine

Pregnancy category: C

Indications

To relieve acute migraine headache
,
Adults. 5 to 10 mg when migraine headache starts; repeated every 2 hr, p.r.n. Maximum: 30 mg daily.
DOSAGE ADJUSTMENT For patients taking propranolol, initial dosage reduced to 5 mg, then repeated every 2 hr, p.r.n., up to maximum of 15 mg daily.

Mechanism of Action

Binds to selective 5-hydroxytryptamine receptor sites on cerebral blood vessels, causing vessels to constrict. This may decrease the characteristic pulsing sensation and thus relieve the pain of migraine headaches. Rizatriptan also may relieve pain by inhibiting the release of proinflammatory neuropeptides and reducing transmission of trigeminal nerve impulses from sensory nerve endings during a migraine attack.

Contraindications

Basilar or hemiplegic migraine, hypersensitivity to rizatriptan or its components, ischemic coronary artery disease, uncontrolled hypertension, use within 14 days of MAO inhibitor therapy, use within 24 hours of other serotonin-receptor agonists or ergotamine-containing or ergot-type

Interactions

ergot-containing : Prolonged vasospastic reactions MAO inhibitors, propranolol: Increased blood rizatriptan level selective serotonin-reuptake inhibitors: Increased risk of weakness, hyperreflexia, and lack of coordination serotonin-receptor agonists: Additive vasospastic effects

Side Efect

CNS: Altered temperature sensation, anxiety, asthenia, ataxia, chills, confusion, depression, disorientation, dizziness, dream disturbances, drowsiness, euphoria, fatigue, hangover, headache, hypoesthesia, insomnia, mental impairment, nervousness, paresthesia, somnolence, tremor, vertigo
CV: Arrhythmias, such as bradycardia and tachycardia; chest pain; hot flashes; hypertension; palpitations
EENT: Blurred vision; burning eyes; dry eyes, mouth, and throat; earache; eye pain or irritation; lacrimation; nasal congestion and irritation; pharyngeal edema; pharyngitis; tinnitus; tongue swelling
GI: Abdominal distention, constipation, diarrhea, dysphagia, flatulence, heartburn, indigestion, nausea, thirst, vomiting
GU: Menstrual irregularities, polyuria, urinary frequency
MS: Arthralgia; dysarthria; muscle spasms, stiffness, or weakness; myalgia
RESP: Dyspnea, upper respiratory tract infection, wheezing
SKIN: Diaphoresis, flushing, pruritus, rash, urticaria
Other: Angioedema, dehydration, facial edema

Cautions

Use rizatriptan cautiously in patients with renal or hepatic dysfunction because of impaired drug metabolism or excretion. Monitor patient’s BUN and serum creatinine levels and liver function test results, as appropriate.

Also use cautiously in patients with rizatriptan benzoate 916 peripheral vascular disease because drug may cause vasospastic reactions, leading to vascular and colonic ischemia with abdominal pain and bloody diarrhea. Assess peripheral circulation and bowel sounds frequently during therapy.

Assess patient’s cardiovascular status and institute continuous ECG monitoring, as ordered, immediately after giving rizatriptan in patients with cardiovascular risk factors because of possible asymptomatic cardiac ischemia.

Monitor blood pressure regularly in patients with hypertension because rizatriptan may increase blood pressure.

PATIENT SAFTY

Instruct patient taking rizatriptan disintegrating tablets to remove tablet from blister pack with dry hands just before taking, to place tablet on tongue, and to allow it to dissolve and be swallowed with saliva.

Advise phenylketonuric patient not to use disintegrating tablet form because it contains phenylalanine.

Instruct patient to seek emergency care immediately if cardiac symptoms, such as chest pain, occur after administration.

Caution patient about possible adverse CNS reactions, and advise her to avoid potentially hazardous activities until drug’s CNS effects are known.

Category

Chemical class: Fc-peptide fusion protein
Therapeutic class: Platelet production enhancer

Pregnancy category: C

Indications

To treat thrombocytopenia in patients with chronic immune (idiopathic) thrombocytopenic purpura (ITP) who have had an insufficient response to corticosteroids, immunoglobulins, or splenectomy SUBCUTANEOUS INJECTION
Adults. Initial: 1 mcg/kg based on actual body weight, followed by weekly doses adjusted in increments of 1 mcg/kg to keep platelet count at or above 50 3 109/L. Maximum: 10 mcg/kg weekly.
DOSAGE ADJUSTMENT If platelet count is less than 50 3 109/L, dosage increased by 1 mcg/kg. If platelet count exceeds 200 3 109/L for 2 consecutive weeks, dosage reduced by 1 mcg/kg. If platelet count exceeds 400 3 109/L, dose held until count has fallen to less than 200 3 109/L and then resumed at a weekly dosage reduced by 1 mcg/kg. Route Onset Peak Duration SubQ Unknown 7–50 hr Unknown

Mechanism of Action

Increases platelet production by binding and activating the thrombopoietin receptor in the same manner as endogenous thrombopoietin to prevent bleeding.

Contraindications

Hypersensitivity to romiplostim or its components

Side Efect

CNS: Dizziness, headache, insomnia, paresthesia
CV: Thrombosis
GI: Abdominal pain, dyspepsia
HEME: Bone marrow reticulin deposition
MS: Arthralgia, extremity or shoulder pain, myalgia
Other: Antibody formation to romiplostim

Cautions

Be aware that romiplostim can be administered only by prescribers or healthcare providers under their direction who are enrolled in the NEXUS program.

Romiplostim therapy is used to reduce the risk of bleeding and not as a therapy to normalize platelet counts.

Be aware that romiplostim may increase patient’s risk for hematologic malignancies.

Obtain a CBC, including platelet count and peripheral blood smears, before starting therapy, weekly until dosage is stable, monthly throughout therapy, and for at least 2 weeks after stopping therapy, as ordered. Detection of peripheral blood cell abnormalities may require a bone marrow examination to identify specific abnormality.

Expect dosage to be adjusted based on weekly platelet count response because, if dosage is too high, thrombotic and thromboembolic complications may occur..

Reconstitute drug using only preservativefree sterile water for injection, adding 0.72 ml to 250-mcg vial or 1.2 ml to 500mcg vial. Gently swirl and invert vial to dissolve powder, which normally occurs within 2 minutes. Don’t shake or agitate vigorously. Protect reconstituted drug from light.

To determine amount of reconstituted drug to administer, first identify patient’s total dose in micrograms based on actual body weight. For example, a patient starting therapy at 1 mcg/kg who weighs 75 kg will receive 75 mcg. Then, divide ordered microgram dose by concentration of reconstituted drug solution (500 mcg/ml). For example, a 75-mcg dose divided by 500 mcg/ml will result in 0.15 ml of drug being administered. Discard any unused portion, and don’t administer more than one dose from a vial because reconstituted drug can only be stored 24 hours, and drug is given only weekly.

Administer drug using a syringe that contains 0.01-ml graduations to ensure accurate dosage because volume to be administered may be quite small.

Be aware that drug may be given with other ITP therapies, such as corticosteroids, danazol, azathioprine, I.V. immunoglobulin and anti-D immunoglobulin.

Expect therapy to be discontinued after 4 weeks at maximum dosage if platelet count doesn’t increase enough to prevent serious bleeding or if patient develops new or worsening abnormalities or cytopenias.

Monitor patient closely for bleeding after drug has been discontinued because thromboyctopenia may occur at greater severity than when therapy was started.

PATIENT SAFTY

Inform patient about increased risk of hematologic malignancies before starting romiplostim therapy.

Stress importance of weekly blood tests to ensure accurate dosing and early detection of serious blood

Side Efect

.

Urge patient to take precautions to prevent bleeding and to avoid aspirin, NSAIDs, and other that may increase bleeding risk.

Instruct patient to seek emergency care immediately if unusual signs and symptoms occur that suggest a blood clot, such as shortness of breath, anxiety, change in skin color or mental status, or development of abnormal sensory or motor function.

When therapy ends, warn patient to report any serious or prolonged bleeding episodes because additional therapy may be needed to control bleeding.

Category

Chemical class: Non-ergot alkaloid dopamine agonist
Therapeutic class: Antidyskinetic

Pregnancy category: C

Indications

To treat signs and symptoms of Parkinson’s disease
Adults. Initial: 0.25 mg t.i.d. Dosage titrated upward every wk according to the following schedule: 0.25 mg t.i.d. in wk 1; 0.5 mg t.i.d. in wk 2; 0.75 mg t.i.d. in wk 3; 1 mg t.i.d. in wk 4. After wk 4, dosage increased by 1.5 mg daily every wk up to 9 mg daily, then by 3 mg/day up to 24 mg daily. Maximum: 24 mg/day.
Adults. Initial: 2 mg once daily for 1 to 2 wk, increased, as needed, in increments of 2 mg/day at 1 wk or longer intervals. Maximum: 24 mg/day. To treat moderate to severe primary restless legs syndrome
Adults. Initial: 0.25 mg 1 to 3 hr before bedtime. Dosage increased after 2 days to 0.5 mg and then to 1 mg at the end of the first wk. If needed, dosage further increased in 0.5-mg increments every wk. Maximum: 4 mg daily.

Mechanism of Action

Directly stimulates postsynaptic dopamine type 2 (D2) receptors within the brain and acts as an agonist at peripheral D2receptors. These actions inhibit the firing of striatal cholinergic neurons, thus helping to control alterations in voluntary muscle movement (such as tremors and rigidity) associated with Parkinson’s disease.

Contraindications

Hypersensitivity to ropinirole or its components

Interactions

carbamazepine, cimetidine, ciprofloxacin, clarithromycin, diltiazem, enoxacin, erythromycin, fluvoxamine, mexiletine, norfloxacin, omeprazole, phenobarbital, phenytoin, rifampin, ritonavir, troleandomycin: Altered drug clearance and increased blood level of ropinirole chlorprothixene, domperidone, droperidol, haloperidol, metoclopramide, phenothiazines, thiothixene: Possibly decreased effectiveness of ropinirole
CNS depressants: Additive effects ethinyl estradiol: Possibly reduced clearance of ropinirole
alcohol use: Additive effects

Side Efect

CNS: Asthenia, confusion, dizziness, falling asleep during activities of daily living, fatigue, hallucinations, headache, hypoesthesia, malaise, neuralgia, paresthesia, rigors, somnolence, syncope, transient ischemic attack, vertigo
CV: Acute coronary syndrome, angina, bradycardia, cardiac failure, chest pain, hypertension, MI, orthostatic hypotension, palpitations, peripheral edema, sick sinus syndrome, tachycardia
EENT: Abnormal vision, dry mouth, nasal congestion, nasopharyngitis, rhinitis, toothache
GI: Abdominal pain, constipation, diarrhea, dyspepsia, gastric hemorrhage, gastroenteritis, indigestion, intestinal obstruction, ischemic hepatitis, nausea, pancreatitis, vomiting
GU: Elevated BUN level, erectile dysfunction, UTI
HEME: Anemia
MS: Arthralgia; arthritis; exacerbation of restless leg syndrome in the early-morning hours; limb pain; muscle cramps, spasms, or stiffness; myalgia; neck pain; osteoarthritis; tendinitis
RESP: Asthma, bronchitis, cough, upper respiratory tract infection
SKIN: Diaphoresis, flushing, hot flashes, night sweats, rash
Other: Influenza, intense urges to perform certain activities (such as gambling or sex), viral infection, weight loss

Cautions

WARNING Expect to reassess patient for excessive sedation periodically during therapy. Excessive, acute drowsiness may arise as late as 1 year after starting therapy.

When ropinirole is given as adjunct to levodopa, expect concurrent dosage of levodopa to be gradually decreased as tolerated.

Expect to stop ropinirole gradually over 7 days, as follows: over first 4 days, reduce from t.i.d to b.i.d.; during last 3 days, reduce to once daily, followed by complete withdrawal of drug.
WARNING Watch for altered mental status during drug withdrawal. Rapid dose reduction may lead to a symptom complex resembling neuroleptic malignant syndrome that includes fever, muscle rigidity, altered level of consciousness, and autonomic instability.

Watch for orthostatic hypotension, especially in patient with early Parkinson’s disease. Orthostatic hypotension can occur more than 4 weeks after start of therapy or after a dosage reduction because ropinirole may impair systemic regulation of blood pressure.

Monitor patient for hallucinations, especially if patient has Parkinson’s disease, is elderly, or takes levodopa.

Monitor patient for worsening of preexisting dyskinesia; ropinirole may potentiate dopaminergic adverse effects of levodopa.

Avoid giving CNS depressants, sleep aids, and other CNS-interacting during ropinirole therapy because they increase the risk of somnolence.

Assess patient for skin changes regularly because risk of melanoma is higher in patients with Parkinson’s disease. It isn’t clear whether this results from disease or used to treat it.

PATIENT SAFTY

Inform patient with Parkinson’s disease that ropinirole helps to improve muscle control and movement but doesn’t cure Parkinson’s disease.

Encourage patient to take ropinirole with food to decrease risk of adverse GI effects.

Caution patient to avoid hazardous activities until CNS effects of drug—including sedation—are known.

If patient falls asleep during normal activities, advise her to notify prescriber.

Urge patient to avoid consuming alcohol and other sedating (such as sleep aids) during therapy because they may increase drug’s CNS depressant effects.

If patient has restless legs syndrome, explain that symptoms might appear in early morning during ropinirole therapy and could be worse or spread to other limbs. Urge patient to notify prescriber if this occurs.

Instruct patient to change positions slowly to minimize effect on blood pressure.

Urge patient to have regular skin examinations by a dermatologist or other qualified health professional.

Advise patient to notify prescriber about intense urges (as for gambling or sex) because dosage may need to be reduced or drug discontinued.

Category

Chemical class: Thiazolidinedione
Therapeutic class: Antidiabetic drug

Pregnancy category: C

Indications

To achieve glucose control in type 2 diabetes mellitus as monotherapy or in combination with metformin
Adults. Initial: 4 mg once daily or 2 mg b.i.d., increased to 8 mg once daily or 4 mg b.i.d. if glucose control is inadequate after 12 wk. Maximum: 8 mg daily. To achieve glucose control in type 2 diabetes mellitus in combination with insulin therapy
Adults. 4 mg daily with no change in insulin dosage. Insulin dosage decreased by 10% to 25% if hypoglycemia occurs or fasting plasma concentrations decrease to less than 100 mg/dl with combination therapy.

Mechanism of Action

Increases tissue sensitivity to insulin. This peroxisome proliferator-activated receptor agonist regulates the transcription of insulin-responsive genes found in key target tissues, such as adipose tissue, skeletal muscle, and the liver. Enhanced tissue sensi-tivity to insulin lowers the blood glucose level.

Contraindications

Hypersensitivity to rosiglitazone or its components, class III or IV heart failure

Interactions

CYP2C8 inducers, such as
rifampin: Possibly decreased effects of rosiglitazone CYP2C8 inhibitors, such as gemfibrozil: Possibly increased effects of rosiglitazone

Side Efect

CNS: Fatigue, headache
CV: Angina, congestive heart failure, edema, hypertension, myocardial ischemia or infarction
EENT: Blurred vision, decreased visual acuity, macular edema, nasopharyngitis, sinusitis
ENDO: Hyperglycemia, hypoglycemia
GI: Diarrhea, elevated liver enzymes, hepatotoxicity
HEME: Anemia
MS: Arthralgia, back pain, fracture (women)
RESP: Dyspnea, upper respiratory tract infection
SKIN: Pruritus, rash, Stevens-Johnson syndrome, urticaria
Other: Anaphylaxis, angioedema, weight gain

Cautions

Give rosiglitazone cautiously in patients with edema, heart failure, or hepatic impairment because of potential adverse reactions.

Be aware that drug isn’t recommended for patients with symptomatic heart failure.

Evaluate patient’s liver function before starting drug and periodically throughout therapy, as ordered. Notify prescriber about abnormalities, such as nausea, vomiting, abdominal pain, fatigue, anorexia, and dark urine. Drug may need to be stopped.
WARNING Monitor patient for evidence of congestive heart failure—such as shortness of breath, rapid weight gain, or edema— because rosiglitazone can cause fluid retention that may lead to or worsen heart failure. Notify prescriber immediately if the patient’s cardiac status deteriorates, and expect to stop the drug, as ordered.

Monitor fasting glucose and glycosylated hemoglobin A1clevels periodically, as ordered, to evaluate rosiglitazone effectiveness.

Be aware that drug is effective only in the presence of endogenous insulin.

PATIENT SAFTY

Stress the need to follow an exercise program and a diet control program during rosiglitazone therapy.

Advise patient to notify prescriber immediately if she has shortness of breath, fluid retention, or sudden weight gain because drug may need to be discontinued.

Instruct patient to have liver function tests, as prescribed, about every 2 months for first year and then annually.

Inform premenopausal, anovulatory patient that drug may induce ovulation, increasing risk of pregnancy.

Urge women to take precautions against falling; drug increases risk of fractures.

Category

Chemical class: HMG-CoA reductase inhibitor
Therapeutic class: Antihyperlipidemic

Pregnancy category: X

Indications

To treat hyperlipidemia, mixed dyslipidemia, hypertriglyceridemia, and primary dysbetalipoproteinemia (Type III hyperlipoproteinemia); to slow the progression of atherosclerosis Adults with LDL-C level of 190 mg/dl or below.Initial: 10 mg daily, increased every 2 to 4 wk, as needed. Maximum: 40 mg daily. Adults with LDL-C level greater than 190 mg/dl. Initial: 20 mg daily, increased every 2 to 4 wk, as needed. Maximum: 40 mg daily. To treat homozygous familial hypercholesterolemia
Adults. Initial: 20 mg daily, increased every 2 to 4 wk, as needed. Maximum: 40 mg daily. To treat heterozygous familial hypercholesterolemia Children age 10 and over and adolescents at least 1 year post-menarche. 5 to 20 mg daily, increased q 4 wk, as needed. Maximum: 20 mg daily.
DOSAGE ADJUSTMENT For patients taking cyclosporine, dosage shouldn’t exceed 5 mg daily. For Asian patients, initial dosage should be limited to 5 mg daily. For patients taking gemfibrozil or combined lopinavir and ritonavir, 10 mg daily. For patients with severe renal impairment (creatinine clearance greater than 30 ml/min/ 1.73 m2) who aren’t having hemodialysis, dosage should start at 5 mg daily but not exceed 10 mg daily. For patients taking niacin or fenofbrate, dosage reduction should be considered. Route Onset Peak Duration P.O. Unknown 3–5 hr Unknown

Mechanism of Action

Cholesterol and triglycerides circulate in the blood as part of lipoprotein complexes. Rosuvastatin inhibits the enzyme 3hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. This inhibition reduces lipid levels by increasing the number of hepatic low-density-lipoprotein (LDL) receptors on the cell surface to increase uptake and catabolism of LDL. It also inhibits hepatic synthesis of very-lowdensity lipoprotein (VLDL), which decreases the total number of VLDL and LDL particles.

Contraindications

Active liver disease, breast-feeding, hypersensitivity to rosuvastatin or its components, pregnancy, unexplained persistent elevations of serum transaminase levels

Interactions

antacids: Decreased blood rosuvastatin level if given within 2 hours of rosuvastatin cyclosporine, gemfibrozil, lopinavir/ritonavir, niacin, other lipid-lowering : Increased rosuvastatin level and risk of myopathy oral contraceptives: Increased blood ethinyl estradiol and norgestrel levels
warfarin: Increased INR

Side Efect

CNS: Asthenia, depression, dizziness, headache, hypertonia, insomnia, memory loss, paresthesia
CV: Chest pain, hypertension, peripheral edema
EENT: Pharyngitis, rhinitis, sinusitis
ENDO: Thyroid function abnormalities
GI: Abdominal pain, constipation, diarrhea, elevated liver function test results, gastroenteritis, hepatic failure, hepatitis, jaundice, nausea, pancreatitis
GU: Acute renal failure, proteinuria, UTI
MS: Arthralgia, arthritis, back pain, myalgia, myopathy, rhabdomyolysis
RESP: Bronchitis, increased cough
SKIN: Rash, urticaria
Other: Angioedema, flulike symptoms, generalized pain, infection

Cautions

Use rosuvastatin cautiously in patients who consume large quantities of alcohol or have a history of liver disease because drug is contraindicated in patients with active liver disease or unexplained persistent elevations of transaminase levels.

Also use cautiously in patients with risk factors for myopathy, such as renal impairment, advanced age, and hypothyroidism.

Obtain baseline liver function test results and expect to monitor them every 3 months for abnormal elevations. Notify prescriber if elevations occur. If ALT or AST levels increase to more than three times the normal range, expect dosage to be reduced or drug discontinued.

Monitor serum lipoprotein level, as ordered, to evaluate response to therapy.

Expect rosuvastatin to be temporarily withheld if patient develops any condition that may be related to myopathy or that predisposes her to renal failure, such as sepsis, hypotension, major surgery, trauma, uncontrolled seizures, or severe metabolic, endocrine, or electrolyte disorders.

Notify prescriber if proteinuria or hematuria appears on patient’s routine urinalysis because rosuvastatin dosage may need to be reduced.

PATIENT SAFTY

Encourage patient to follow a low-fat, lowcholesterol diet.

Tell patient to wait at least 2 hours after taking rosuvastatin before taking antacids.

Instruct patient to notify prescriber immediately about muscle pain, tenderness, or weakness, especially if accompanied by malaise or fever.

Tell woman of childbearing age about the need to use reliable contraceptive method while taking drug. Instruct her to notify prescriber at once if she suspects she may be pregnant.

Category

Chemical class: Triazole derivative
Therapeutic class: Anticonvulsant

Pregnancy category: C

Indications

As adjunct treatment of seizures associated with Lennox-Gastaut syndrome
Adults. Initial: 200 to 400 mg b.i.d., increased in daily increments of 200 to 400 mg b.i.d. every 2 days until reaching 1,600 mg b.i.d. Maximum: 1,600 mg b.i.d. Children age 4 and over.Initial: 5 mg/kg b.i.d., increased in daily increments of 5 mg/kg b.i.d. every 2 days until reaching 22.5 mg/kg b.i.d. or 1600 mg b.i.d., whichever is less.
DOSAGE ADJUSTMENT For patients undergoing dialysis, dosage may need to be increased. For patients also receiving valrufinamide 922 proate, initial dosage reduced to less than 400 mg daily. Route Onset Peak Duration P.O. Unknown 4–6 hr Unknown

Mechanism of Action

Unknown, although rufinamide is known to slow sodium channel recovery from inactivation after a prolonged prepulse and to limit repetitive firing of sodium-dependent action potentials in neurons in the brain. These actions may help limit seizure activity.

Contraindications

Familial short-QT syndrome, hypersensitivity to rufinamide or its components

Interactions

contraceptives containing ethinyl estradiol and norethindrone: Decreased effectiveness of the oral contraceptive
phenytoin: Increased plasma phenytoin level and risk of

Side Efect

valproate: Increased plasma rufinamide level and risk of

Side Efect

alcohol use: Increased CNS effects

Side Efect

CNS: Aggression, anxiety, ataxia, attention disturbance, dizziness, fatigue, headache, hyperactivity, seizures, somnolence, status epilepticus, suicidal ideation, tremor, vertigo
CV: First-degree AV block, right bundle branch block
EENT: Sinusitis
ENDO: Blurred vision, diplopia, nasopharyngitis, nystagmus
GI: Abdominal pain, anorexia, constipation, dyspepsia, nausea, vomiting
GU: Dysuria, enuresis, hematuria, incontinence, nephrolithiasis, pollakiuria, polyuria
HEME: Anemia, leukopenia, lymphadenopathy, neutropenia, thrombocytopenia
MS: Back pain
RESP: Bronchitis
SKIN: Pruritus, rash
Other: Multi-organ hypersensitivity

Cautions

Administer rufinamide with food because absorption is increased.

Monitor patient’s QT interval regularly, as ordered, because rufinamide may shorten the QT interval and possibly predispose patient to ventricular fibrillation if the interval falls below 300 msec.
WARNING Watch closely for multi-organ hypersensitivity, especially if patient develops a rash. Although uncommon, it may cause serious adverse effects, such as urticaria, facial edema, fever, elevated eosinophils or liver enzymes, hematuria, stupor, lymphadenopathy and severe hepatitis, in addition to rash. Notify prescriber at once if such changes appear, and expect to stop drug and provide supportive care.

Watch closely for suicidal tendencies, especially when therapy starts and dosage changes and particularly in children and adolescents.

To stop therapy, expect to taper dosage to minimize adverse effects rather than stopping abruptly.

PATIENT SAFTY

Make sure patient receives medication guide describing drug use and possible suicidal tendencies.

Instruct patient to take drug exactly as prescribed and to take each dose with food. If patient has trouble swallowing tablets, tell him they may be crushed.

Inform woman that rufinamide decreases effectiveness of contraceptives containing ethinyl estradiol and norethindrone. Tell her to use a different contraceptive during therapy and to contact prescriber immediately if she thinks she’s pregnant.

Tell patient to report a rash accompanied by fever or other symptoms immediately.

Warn family or caregiver to watch patient for suicidal tendencies, especially when therapy starts or dosage changes, and particularly if patient is a child or adolescent.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Caution patient not to stop taking drug abruptly. Explain that gradual tapering helps to avoid withdrawal symptoms.

Explain that alcohol consumption may intensify drug effects.

Category

Chemical class: Sympathomimetic amine
Therapeutic class: Bronchodilator

Pregnancy category: C

Indications

To prevent asthma-induced bronchospasm ORAL INHALATION POWDER Adults and children age 4 and over. 1 inhalation (50 mcg) every 12 hr. To prevent COPD-induced bronchospasm ORAL INHALATION POWDER
Adults. 1 inhalation (50 mcg) every 12 hr. To prevent exercise-induced bronchospasm ORAL INHALATION POWDER Adults and children age 4 and over. 1 inhalation (50 mcg) at least 30 min before exercise. Route Onset Peak Duration Inhalation 10–20 min 3–4 hr 12 hr

Mechanism of Action

Attaches to beta2receptors on bronchial cell membranes, stimulating the intracellular enzyme adenylate cyclase to convert adenosine triphosphate to cAMP. The resulting increase in intracellular cAMP level relaxes bronchial smooth-muscle cells, stabilizes mast cells, and inhibits histamine release.

Contraindications

Hypersensitivity to salmeterol or its components

Interactions

atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin: Possibly increased risk of adverse cardiovascular effects
beta blockers: Mutual inhibition of therapeutic effects loop or thiazide diuretics: Increased risk of hypokalemia and potentially life-threatening arrhythmias MAO inhibitors, tricyclic antidepressants: Potentiated adverse vascular effects, such as hypertensive crisis

Side Efect

CNS: Dizziness, fever, headache, nervousness, paresthesia, tremor
CV: Palpitations, tachycardia
EENT: Dry mouth, nose, and throat; sinus problems
GI: Nausea
MS: Arthralgia
RESP: Cough, paradoxical bronchospasm
SKIN: Contact dermatitis, eczema, rash, urticaria
Other: Angioedema, generalized aches and pains

Cautions

Be aware that salmeterol shouldn’t be used to relieve bronchospasm quickly because of its prolonged onset of action and that patients already taking drug twice daily shouldn’t take additional doses for exercise-induced bronchospasm.
WARNING Be aware that a recent study suggests that asthma-related deaths may increase in asthmatics receiving salmeterol. Monitor this patient population closely throughout salmeterol therapy, and notify prescriber immediately of any changes in patient’s respiratory status.

Watch for arrhythmias and changes in blood pressure after use in patients with cardiovascular disorders, including ischemic cardiac disease, hypertension, and arrhythmias, because of drug’s betaadrenergic effects.

Be aware that Serevent Diskus delivers full dose of salmeterol in only one inhalation.
WARNING Stop salmeterol immediately and notify prescriber if patient develops paradoxical bronchospasm. Risk is greatest with first use of a new canister or vial used as an inhalant.

PATIENT SAFTY

Advise patient who is using salmeterol to prevent asthma-induced bronchospasm to take doses 12 hours apart for optimum effect. Caution against using drug more than every 12 hours.

Teach patient how to use the diskus by instructing him to slide the lever only once when preparing dose to avoid wasting doses. Advise him to exhale immediately before using the diskus and then to place mouthpiece to his lips and inhale through his mouth, not his nose. Then he should remove mouthpiece from his mouth, hold his breath for at least 10 secsalmeterol xinafoate 924 onds, and exhale slowly.

Advise patient to rinse mouth with water after each dose to minimize dry mouth.

Advise patient to discard diskus 6 weeks after removing it from overwrap or when dose indicator reads zero.

Instruct patient to notify prescriber if he needs four or more oral inhalations of rapid-acting inhaled bronchodilator a day for 2 or more consecutive days, or if he uses more than one canister of rapid-acting bronchodilator in an 8-week period.

Caution patient not to use other to treat his underlying respiratory condition without consulting prescriber and to let all prescribers know that he takes salmeterol.

Category

Chemical class: Salicylic acid ester
Therapeutic class: Analgesic, antiinflammatory

Pregnancy category: C

Indications

To relieve symptoms of rheumatoid arthritis and related rheumatic disorders Adults and adolescents. Initial: 1 g t.i.d.; dosage then titrated, as needed. Adults and adolescents. Initial: 0.5 to 1 g b.i.d. or t.i.d.; dosage then titrated, as needed. Route Onset Peak Duration P.O. Unknown 2–3 wk Unknown

Mechanism of Action

Exerts peripherally induced analgesic and anti-inflammatory effects by blocking pain impulses and inhibiting prostaglandin synthesis.

Contraindications

Bleeding disorders; hypersensitivity to NSAIDs, salicylates, or their components

Interactions

acetaminophen: Increased risk of renal dysfunction with prolonged use of both anticoagulants, thrombolytics: Increased risk and severity of GI bleeding antiemetics: Masked symptoms of salicylateinduced ototoxicity bismuth subsalicylate: Increased risk of salicylate toxicity with large doses of salsalate cefamandole, cefoperazone, cefotetan, platelet aggregation inhibitors, plicamycin,
valproic acid: Possibly hypoprothrombinemia corticosteroids: Possibly decreased blood salsalate level; additive therapeutic effects when both are used to treat arthritis furosemide: Increased risk of ototoxicity and salicylate toxicity hydantoins: Possibly decreased hydantoin metabolism, leading to toxicity insulin, oral antidiabetic : Potentiated hypoglycemic effect laxatives (cellulose-containing): Possibly reduced salsalate effectiveness due to impaired absorption methotrexate: Increased risk of methotrexate toxicity
NSAIDs: Increased risk of adverse GI effects ototoxic , vancomycin: Increased risk of ototoxicity probenecid, sulfinpyrazone: Decreased uricosuric effects topical salicylic acid, other salicylates: Increased risk of salicylate toxicity if significant quantities are absorbed urinary acidifiers (ammonium chloride, ascorbic acid, potassium or sodium phosphates): Decreased salicylate excretion, possibly leading to salicylate toxicity urinary alkalizers (antacids [long-term highdose use], carbonic anhydrase inhibitors, citrates, sodium bicarbonate): Increased salicylate excretion, leading to reduced effectiveness and shortened half-life; increased risk of salicylate toxicity with carbonic anhydrase inhibitor–induced metabolic acidosis vitamin K: Increased vitamin K requirements
alcohol use: Increased risk of GI bleeding

Side Efect

CNS: CNS depression, confusion, dizziness, drowsiness, fever, headache, lassitude
EENT: Hearing loss, tinnitus, vision changes
GI: Anorexia, diarrhea, epigastric discomfort, GI bleeding, heartburn, hepatotoxicity, indigestion, nausea, thirst, vomiting
HEME: Hemolytic anemia, leukopenia, prolonged bleeding time, thrombocytopenia
SKIN: Diaphoresis, purpura, rash, urticaria
Other: Angioedema, Reye’s syndrome

Cautions

Avoid using salsalate in patients with hypoprothrombinemia or vitamin K deficiency because drug’s hypoprothrombinemic effect may precipitate bleeding.

Monitor hepatic and renal function, as appropriate, during long-term therapy.

Assess for signs and symptoms of GI bleeding, such as abdominal pain or black, tarry stools, especially in patient with peptic ulcer disease.

Assess for symptoms of ototoxicity, such as ringing or roaring in ears.

PATIENT SAFTY

Instruct patient to take salsalate with food or a full glass of water and to remain upright for 1 hour after administration to prevent drug from lodging in esophagus and causing irritation.

Inform patient that therapeutic response may not occur for 2 to 3 weeks.

Urge patient to notify prescriber immediately of abdominal pain or black, tarry stools; these symptoms may indicate GI bleeding or drug toxicity.

Category

Chemical class: Synthetic tetrahydrobiopterin salt
Therapeutic class: Phenylalanine reducer

Pregnancy category: C

Indications

To reduce blood phenylalanine level in patients with hyperphenylalaninemia from tetrahydrobiopterin-responsive phenylketonuria, with phenylalaninerestricted diet Adults and children age 4 and over. Initial: 10 mg/kg daily with dosage increased or decreased after 1 wk based on response and then periodically adjusted, as needed. Expect to discontinue drug if levels fail to increase after 1 mo of therapy at 20 mg/kg/day. Maintenance: 5 to 20 mg/kg daily. Maximum: 20 mg/kg daily.

Mechanism of Action

As a synthetic form of tetrahydrobiopterin, the cofactor of the enzyme phenylalanine hydroxylase (PAH), sapropterin hydroxylates phenylalanine to form tyrosine. This improves the oxidative metabolism of phenylalanine, which decreases blood phenylalanine.

Contraindications

Hypersensitivity to sapropterin or its components

Interactions

folate metabolism inhibitors, such as methotrexate: Possibly decreased effectiveness of sapropterin levodopa: Possibly increased risk of irritability, over stimulation or seizures sildenafil, tadalafil, vardenafil: Possibly additive vasorelaxation effect leading to hypotension

Side Efect

CNS: Agitation, dizziness, fever, headache, irritability, over stimulation, seizures
CV: MI, peripheral edema
EENT: Nasal congestion, pharyngolaryngeal pain, rhinorrhea
GI: Abdominal pain, diarrhea, elevated liver enzymes, gastrointestinal bleeding, nausea, vomiting
GU: Polyurina
HEME: Bleeding, neutropenia
MS: Arthralgia
RESP: Cough, respiratory failure, upper respiratory infection
SKIN: Rash

Cautions

Use cautiously in patients with hepatic impairment because impaired phenylalanine metabolism may be linked to hepatic damage.

Administer drug at same time each day.

Dissolve tablets in 4 to 8 ounces of water or apple juice, which may take a few minutes. Stirring or crushing tablets will hasten process. Know that tablets may not dissolve completely. Give solution within 15 minutes with food. If there are particles left in glass after administration, add more water or apple juice and have patient drink again to ensure a complete dose.

Monitor patient’s blood phenylalanine level regularly, as ordered.

Expect drug to be discontinued if patient’s blood phenylalanine level doesn’t decrease after 1 month at maximum dosage.

Continue to restrict dietary phenylalanine intake.

PATIENT SAFTY

Tell patient to dissolve tablets in 4 to 8 ounces water or apple juice, which may take a few minutes. Advise him to stir or crush tablets to hasten process and to drink solution within 15 minutes of dissolving. Explain that tablets may not completely dissolve but that solution is alright to drink with particles floating in solution. After drinking solution, tell him to add more water or apple juice if any particles are clinging to glass and drink again.

Stress to patient or caregiver importance of continuing dietary restriction of phenylalanine intake.

Stress continued need for periodic blood tests to determine drug effectiveness.

Tell patient to a missed dose as soon as he remembers, unless it’s almost time for the next dose. Warn patient not to take more than 1 dose per day.

Category

Chemical class: Dipeptidyl peptidase-4 inhibitor
Therapeutic class: Antidiabetic

Pregnancy category: B

Indications

To improve blood glucose control in type 2 diabetes mellitus as adjunct to diet and exercise
Adults. 2.5 mg or 5 mg once daily
DOSAGE ADJUSTMENT For patients with moderate or severe renal impairment (creatinine clearance 50 ml/min/1.73 m2or less), patients with end-stage renal disease, patients having hemodialysis, and patients receiving strong CYP3A4/5 inhibitors, dosage shouldn’t exceed 2.5 mg once daily. Route Onset Peak Duration P.O. Unknown 2 hr 24 hr

Mechanism of Action

Incretin hormones, such as glucosedependent insulintropic polypeptide (GIP) and glucagons-like peptide-1 (GLP-1), are released into bloodstream from small intestine in response to meals. Upon arrival at the pancreas, they stimulate pancreatic beta cells to release insulin. GLP-1 also reduces glucagon secretion from pancreatic alpha cells, which reduces hepatic glucose production. Incretin hormones become inactivated within minutes of release by the enzyme, dipeptidyl peptidase-4. Saxagliptin inhibits this enzyme, thereby slowing inactivation of incretin hormones, which provides more time for them to increase insulin levels and blunt glucagon secretion. More insulin and less hepatic glucose production work together to lower blood glucose levels.

Contraindications

Hypersensitivity to saxagliptin or its components

Interactions

aprepitant, diltiazem, erythromycin, fluconazole, fosamprenavir, verapamil: Possibly increased plasma saxagliptin level atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin: Increased plasma saxagliptin level sulfonylureas: Increased risk of hypoglycemia grapefruit juice: Possibly increased plasma saxagliptin levels

Side Efect

CNS: Headache
EENT: Sinusitis, nasopharyngitis
ENDO: Hypoglycemia
GI: Abdominal pain, gastroenteritis, vomiting
GU: Elevated plasma creatinine level, UTI
HEME: Lymphopenia
RESP: Upper respiratory tract infection
SKIN: Rash, urticaria
Other: Peripheral edema, facial edema

Cautions

Saxagliptin shouldn’t be used to treat type 1 diabetes mellitus or diabetic ketoacidosis. It hasn’t been studied with insulin.

Obtain a serum creatinine level, as ordered, before starting saxagliptin therapy and then periodically thereafter to monitor patient’s renal function.

Monitor patient’s blood glucose level and hemoglobin A1Cto assess effectiveness of saxagliptin therapy.

Watch for hypoglycemia in patients taking antidiabetics, such as sulfonylureas. Expect dosage of insulin secretagogues (such as sulfonylureas) to be reduced to reduce risk of hypoglycemia.

PATIENT SAFTY

Stress that saxagliptin isn’t a replacement for diet and exercise therapy.

Explain importance of self-monitoring glucose levels during saxagliptin therapy.

Teach patient to recognize hypoglycemia and how to treat it if it should occur. Urge him to carry glucose with him at all times in case hypoglycemia occurs.

Instruct patient to notify prescriber if fever, trauma, infection, illness, surgery, or other stress occurs because blood glucose control may be altered requiring temporary insulin therapy.

Category

Chemical class: Belladonna alkaloid, tertiary amine
Therapeutic class: Anesthesia adjunct, anticholinergic, antiemetic, antispasmodic, anti-vertigo

Pregnancy category: C

Indications

To treat biliary tract disorders, enuresis, nausea and vomiting, and nocturia I.V., I.M., OR SUBCUTANEOUS INJECTION (HYDROBROMIDE) Adults and adolescents. 300 to 600 mcg (0.3 to 0.6 mg) as a single dose. Children. 6 mcg (0.006 mg)/kg as a single dose. To prevent excessive salivation and respiratory tract secretions during anesthesia
I.M.INJECTION(HYDROBROMIDE) Adults and adolescents. 0.2 to 0.6 mg 30 to 60 min before induction of anesthesia. Children ages 8 to 12. 0.3 mg 45 to 60 min before induction of anesthesia. Children ages 3 to 8. 0.2 mg 45 to 60 min before induction of anesthesia. Children ages 7 months to 3 years. 0.15 mg 45 to 60 min before induction of anesthesia. Infants ages 4 to 7 months.0.1 mg 45 to 60 min before induction of anesthesia. As adjunct to anesthesia to induce sleep and calmness I.V., I.M., OR SUBCUTANEOUS INJECTION (HYDROBROMIDE) Adults and adolescents. 0.6 mg t.i.d. or q.i.d. As adjunct to anesthesia to induce amnesia I.V., I.M., OR SUBCUTANEOUS INJECTION (HYDROBROMIDE) Adults and adolescents. 0.32 to 0.65 mg. To prevent nausea, vomiting, and vertigo associated with motion sickness TRANSDERMAL SYSTEM Adults and adolescents. 1 U.S. transdermal system (0.5 mg) applied behind ear for 3day period, beginning at least 4 hr before antiemetic effect is required. Or, 1 Canadian transdermal system (1 mg) applied behind ear for 3-day period, beginning at least 12 hr before antiemetic effect is required.
DOSAGE ADJUSTMENT Dosage reduction possible for elderly patients because of their increased sensitivity to scopolamine.

Contraindications

Angle-closure glaucoma; hemorrhage with hemodynamic instability; hepatic dysfunction; hypersensitivity to barbiturates, scopolamine, other belladonna alkaloids, or their components; ileus; intestinal atony; myasthenia gravis; myocardial ischemia; obstructive GI disease, such as pyloric stenosis; obstructive uropathy, as in prostatic hyperplasia; renal impairment; tachycardia; toxic megacolon; ulcerative colitis Route Onset Peak Duration I.V.,I.M., 30 min 1–2 hr 4–6 hr SubQ* I.V. 10 min 50–80 min 2 hr I.M. 15–30 Unknown 4 hr min Trans4 hr Unknown 72 hr dermal

Mechanism of Action

Competitively inhibits acetylcholine at autonomic postganglionic cholinergic receptors. Because the most sensitive receptors are in the salivary, bronchial, and sweat glands, this action reduces secretions from these glands. Scopolamine reduces GI smooth-muscle tone; decreases gastric secretions and GI motility; reduces bladder detrusor muscle tone; reduces nasal, oropharyngeal, and bronchial secretions; and decreases airway resistance by relaxing smooth muscles in the bronchi and bronchioles. Scopolamine also blocks neural pathways in the inner ear to relieve motion sickness and depresses the cerebral cortex to produce sedation and hypnotic effects.

Interactions

adsorbent antidiarrheals, antacids: Decreased absorption and therapeutic effects of scopolamine anticholinergics (other): Possibly intensified anticholinergic effects antimyasthenics: Possibly reduced intestinal motility
CNS depressants: Possibly potentiated effects of either drug, resulting in additive sedation cyclopropane: Increased risk of ventricular arrhythmias (with I.V. scopolamine)
haloperidol: Decreased antipsychotic effect of haloperidol
ketoconazole: Decreased ketoconazole absorption lorazepam (parenteral): Possibly hallucinations, irrational behavior, and sedation metoclopramide: Possibly antagonized effect of metoclopramide on GI motility opioid analgesics: Increased risk of severe constipation and ileus potassium chloride: Possibly increased severity of potassium chloride–induced GI lesions urinary alkalizers (antacids, carbonic anhydrase inhibitors, citrates, sodium bicarbonate): Delayed excretion of scopolamine, possibly leading to increased therapeutic and adverse effects
alcohol use: Additive CNS effects

Side Efect

CNS: Dizziness, drowsiness, euphoria, insomnia, memory loss, paradoxical stimulation
CV: Palpitations, tachycardia
EENT: Blurred vision; dry eyes, mouth, nose, and throat; mydriasis
GI: Constipation, dysphagia
GU: Urinary hesitancy, urine retention
SKIN: Decreased sweating, dry skin, flushing
Other: Injection site irritation or redness

Cautions

For I.V. injection, dilute scopolamine with sterile water for injection.

Assess for bladder distention and monitor urine output because drug’s antimuscarinic effects can cause urine retention.

Monitor for pain. In presence of pain, drug may act as a stimulant and produce delirium if used without morphine or meperidine.

Monitor heart rate for transient tachycardia, which may occur with high doses of drug. Rate should return to normal within 30 minutes.

PATIENT SAFTY

Instruct patient to apply scopolamine transdermal patch on hairless area behind * For inhibition of saliva. For amnesia. For antiemesis. ear and to wash hands thoroughly with soap and water before and after applying.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to avoid alcohol while taking oral forms of scopolamine.

If patient complains of dry eyes, suggest lubricating drops.

Category

Chemical class: Barbiturate
Therapeutic class: Sedative-hypnotic

Pregnancy category: D

Controlled substance schedule: II

Indications

To induce sedation before surgery
Adults. 200 to 300 mg 1 to 2 hr before surgery. Children. 2 to 6 mg/kg 1 to 2 hr before surgery. Maximum: 100 mg. To provide short-term treatment of insomnia
Adults. 100 mg at bedtime. To relieve apprehension, daytime anxiety, and tension
Adults. 30 to 50 mg t.i.d. or q.i.d. Children. 2 mg/kg t.i.d.
DOSAGE ADJUSTMENT Reduced dosage required for elderly or debilitated patients and those with renal or hepatic dysfunction. Route Onset Peak Duration P.O. 10–15 min 15–30 min 1–4 hr

Mechanism of Action

Inhibits upward conduction of nerve impulses to the reticular formation of the brain, thereby disrupting impulse transmission to the cortex. This action depresses the CNS, producing drowsiness, hypnosis, and sedation.

Contraindications

History of barbiturate addiction; hypersensitivity to secobarbital, other barbiturates, or their components; nephritis; porphyria; severe hepatic or respiratory impairment

Interactions

acetaminophen, adrenocorticoids, beta blockers, chloramphenicol, cyclosporine, dacarbazine, digoxin, disopyramide, estrogens, metronidazole, oral anticoagulants, oral contraceptives, quinidine, thyroid hormones, tricyclic antidepressants: Decreased effectiveness of these addictive : Increased risk of addiction calcium channel blockers: Possibly excessive hypotension carbamazepine, succinimide anticonvulsants: Decreased blood levels and increased elimination of these carbonic anhydrase inhibitors: Increased risk of osteopenia
CNS depressants: Increased CNS depressant effects cyclophosphamide: Increased risk of leukopenic activity and reduced half-life of cyclophosphamide divalproex sodium,
valproic acid: Increased CNS depression and neurologic toxicity doxycycline, fenoprofen: Increased elimination of these general anesthetics (enflurane, halothane, methoxyflurane): Increased risk of hepatotoxicity; increased risk of nephrotoxicity (with methoxyflurane) griseofulvin: Decreased griseofulvin absorption guanadrel, guanethidine: Possibly increased orthostatic hypotension
haloperidol: Possibly altered pattern or frequency of seizures, decreased blood haloperidol level ketamine: Increased risk of hypotension or respiratory depression (when secobarbital is used as preanesthetic) leucovorin (large doses): Decreased anticonvulsant effect of secobarbital loxapine, phenothiazines,
thioxanthenes: Possibly lowered seizure threshold
MAO inhibitors: Possibly prolonged CNS depressant effects of secobarbital maprotiline: Increased CNS depressant effect; possibly lowered seizure threshold and decreased anticonvulsant effect with high doses of maprotiline
methylphenidate: Increased risk of barbitusecobarbital sodium 930 rate toxicity
mexiletine: Decreased blood mexiletine level phenylbutazone: Decreased effectiveness of secobarbital posterior pituitary hormones: Increased risk of arrhythmias and coronary insufficiency primidone: Increased sedative effect of either drug, change in seizure pattern
vitamin D: Decreased vitamin D effects xanthines (aminophylline, oxtriphylline, theophylline): Increased metabolism of xanthines (except dyphylline), decreased hypnotic effect of secobarbital caffeine: Increased caffeine metabolism, decreased hypnotic effect of secobarbital
alcohol use: Increased CNS depression

Side Efect

CNS: Anxiety, clumsiness, confusion, depression, dizziness, drowsiness, hangover, headache, insomnia, irritability, lethargy, nervousness, nightmares, paradoxical stimulation, syncope
CV: Hypotension
EENT: Laryngospasm
GI: Anorexia, constipation, nausea, vomiting
MS: Arthralgia, muscle weakness
RESP: Apnea, bronchospasm, respiratory depression
SKIN: Jaundice
Other: Drug dependence, weight loss

Cautions

Be aware that prolonged use of secobarbital may lead to tolerance and physical and psychological dependence.
WARNING To avoid withdrawal symptoms, expect to taper drug after long-term therapy. Withdrawal symptoms usually appear 8 to 12 hours after stopping drug and may include anxiety, insomnia, muscle twitching, nausea, orthostatic hypotension, vomiting, weakness, and weight loss. Severe symptoms may include delirium, hallucinations, and seizures. Generalized tonicclonic seizures may occur within 16 hours or up to 5 days after last dose.

Assess patient for signs and symptoms of barbiturate toxicity, including dyspnea, severe confusion, and severe drowsiness. Notify prescriber immediately if they appear because barbiturate toxicity may be life-threatening.

Expect prescriber to provide patient with the least possible quantity of secobarbital to minimize the risk of acute or chronic overdosage. For patients who are depressed, suicidal, or drug-dependent or who have a history of drug abuse, institute precautions to prevent drug hoarding and overdosage.

PATIENT SAFTY

Instruct patient to take secobarbital exactly as prescribed because of the risk of addiction.

Inform patient that taking drug with food may reduce adverse GI effects.

Advise patient to avoid alcohol and caffeine and potentially hazardous activities during therapy.

Inform patient about possible hangover effect.

If patient takes an oral contraceptive, recommend using an additional form of birth control during therapy.

Caution patient not to stop taking drug abruptly.

Instruct patient to notify prescriber of bone pain, muscle weakness, or unexplained weight loss during therapy.

Category

Chemical class: Phenethylamine derivative
Therapeutic class: Antidepressant (Emsam), antidyskinetic

Pregnancy category: C

Indications

As adjunct to carbidopa-levodopa therapy to treat Parkinson’s disease ,
Adults. 10 mg once daily, or 5 mg b.i.d. with breakfast and lunch.
DOSAGE ADJUSTMENT For patient with levodopa-induced adverse effects, 2.5 mg q.i.d. As adjunct to carbidopa-levodopa therapy to treat Parkinson’s disease in patients whose response to therapy has deteriorated ORALLY
(ZELAPAR)
Adults. Initial: 1.25 mg once daily before breakfast for at least 6 wk; then increased to 2.5 mg once daily, if needed. To treat depression TRANSDERMAL SYSTEM(EMSAM)
Adults. Initial: 6 mg/24 hr with patch applied daily to upper torso, upper thigh, or outer surface of upper arm. Increased every 2 wk in increments of 3 mg/24 hr, as needed. Maximum: 12 mg/24 hr.

Mechanism of Action

Reduces dopamine metabolism by noncompetitively inhibiting the brain enzyme monoamine oxidase type B. This increases the amount of dopamine available to relieve symptoms of parkinsonism. Selegiline’s metabolites may also enhance dopamine transmission by inhibiting its reuptake at synapses.

Contraindications

Hypersensitivity to selegiline or its components; pheochromocytoma; use within 14 days of meperidine; use within 10 days of general anesthesia; use with carbamazepine, oxcarbazepine, selective serotonin reuptake inhibitors (fluoxetine, paroxetine, sertraline), dual serotonin and norephinephrine reuptake inhibitors (duloxetine, venlafaxine), tricyclic antidepressants (amitriptyline, bupropion, imipramine), analgesics (tramadol, propoxyphene), dextromethorphan; use with St. John’s wort, mirtazapine, cyclobenzaprine, oral selegline, other MAO inhibitors, sympathomimetic amines (Emsam only)

Interactions

carbamazepine, oxcarbazepine: Increased blood selegiline level fluoxetine, fluvoxamine, nefazodone, paroxetine, sertraline, venlafaxine: Increased risk of

Side Efect

similar to those of serotonin syndrome (confusion, hypomania, restlessness, myoclonus), autonomic instability, delirium, muscle rigidity, and severe agitation levodopa: Increased risk of confusion, dyskinesia, hallucinations, nausea, and orthostatic hypotension meperidine, possibly other opioid agonists: Increased risk of diaphoresis, excitation, muscle rigidity, and severe hypertension sympathomimetics: Increased risk of severe hypertension tricyclic antidepressants: Possibly serious CNS reactions, including decreased level of consciousness, hyperpyrexia, hypertension, muscle rigidity, seizures, and syncope caffeine: Increased risk of hypertension that contain tyramine or other highpressor amines: Increased risk of sudden and severe hypertension
alcohol use: Increased risk of hypertension

Side Efect

CNS: Anxiety, chills, confusion, dizziness, drowsiness, dyskinesia, euphoria, extrapyramidal reactions, fatigue, hallucinations, headache, insomnia, irritability, lethargy, memory loss, mood changes, nervousness, paresthesia, restlessness, suicidal ideation, syncope, tremor, weakness
CV: Arrhythmias, chest pain, hypertension, orthostatic hypotension, palpitations, peripheral edema
EENT: Altered taste, blepharospasm, blurred vision, burning lips or mouth, diplopia, dry mouth, pharyngitis, sinusitis, tinnitus
GI: Abdominal pain, anorexia, constipation, diarrhea, GI bleeding, heartburn, nausea, vomiting
GU: Dysuria, urinary hesitancy, urinary urgency, urine retention
MS: Arthralgia, back and leg pain, muscle fatigue and spasms, neck stiffness
RESP: Asthma
SKIN: Diaphoresis, photosensitivity, rash
Other: Application site reactions (Emsam), intense urges to perform certain activities (such as gambling or sex)

Cautions

Assess patient for mental status and mood changes because selegiline can worsen such conditions as dementia, severe psychosis, tardive dyskinesia, and tremor. Be especially alert for suicidal tendencies, particularly when therapy starts or dosage changes.

Monitor patient who is also taking levodopa for levodopa-induced adverse reactions, including confusion, dyskinesia, hallucinations, nausea, and orthostatic hypotension.

Monitor for decreased symptoms of Parkinson’s disease to evaluate drug’s effectiveness.

Be aware that drug can reactivate gastric ulcers because it prevents breakdown of gastric histamine. Assess for related signs and symptoms, such as abdominal pain.

Assess patient for skin changes regularly because risk of melanoma is increased in patients with Parkinson’s disease. It isn’t clear whether increase results from disease or used to treat it.

PATIENT SAFTY

Caution patient to take only prescribed amount because increased dosage may cause severe

Side Efect

.

Advise patient to avoid taking selegiline in the late afternoon or evening because it may interfere with sleep.

For orally
, tell patient to take it before breakfast without any liquid. Caution him not to push tablet through the foil on the blister pack but instead to peel back the foil with dry hands and gently remove the tablet. He should then immediately place the tablets on top of his tongue and let it disintegrate. Advise him not to drink or ingest any food for 5 minutes before and after taking the drug.

If patient will use transdermal form, explain how and where to apply patch, stressing need to rotate sites. Tell patient to wash hands well after application and to dispose of removed patch immediately.

Stress that only one patch may be worn at a time. If a patch falls off, tell patient to apply a new patch to a new site and to resume previous schedule.

Urge patient to avoid tyramine-rich and beverages during and for 2 weeks after stopping selegiline therapy unless patient is prescribed the lowest dosage of transdermal system (6 mg per 24 hours), which doesn’t require diet modification. Review which are considered tyramine-rich.

Instruct patient to immediately report severe headache, neck stiffness, racing heart, palpitations, or other sudden or unusual symptoms.

Caution patient to avoid exposing transdermal patch to sources of direct heat, such as heating pads, electric blankets, heat lamps, saunas, hot tubs, and prolonged sunlight exposure.

Tell patient not to cut transdermal patch into smaller pieces.

Urge caregiver to monitor patient closely for suicidal tendencies, especially when therapy starts or dosage changes.

Urge patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to change positions slowly to minimize the effects of orthostatic hypotension.

Suggest that patient elevate his legs when sitting to reduce ankle swelling.

Urge patient to avoid excessive sun exposure.

Instruct patient to notify prescriber if symptoms develop that could indicate overdose, including muscle twitching and eye spasms.

Urge patient to notify prescriber if dry mouth lasts longer than 2 weeks. Advise him to have routine dental checkups.

Urge patient to have regular skin examinations done by a dermatologist or other qualified health professional.

Advise patient to notify prescriber about intense urges (as for gambling or sex) because dosage may need to be reduced or drug discontinued.

Category

Chemical class: Naphthylamine derivative
Therapeutic class: Antidepressant, antiobsessant, antipanic

Pregnancy category: C

Indications

To treat major depression ORAL CONCENTRATE,
Adults. Initial: 50 mg daily, increased after several wk in increments of 50 mg daily every wk, as needed. Maximum: 200 mg daily. To treat obsessive-compulsive disorder ORAL CONCENTRATE, Adults and adolescents. Initial: 50 mg daily, increased after several wk in increments of 50 mg daily every wk, as needed. Maximum: 200 mg daily. Children ages 6 to 12. Initial: 25 mg daily, increased every wk, as needed. Maximum: 200 mg daily. To treat panic disorder, with or without agoraphobia; to treat posttraumatic stress disorder ORAL CONCENTRATE,
Adults. Initial: 25 mg daily, increased to 50 mg daily after 1 wk; then increased by 50 mg daily every wk, as needed. Maximum: 200 mg daily.
DOSAGE ADJUSTMENT Initial dosage reduction recommended for elderly patients and those with hepatic impairment. To treat premenstrual dysphoric disorder (PMDD) ORAL CONCENTRATE, Adult women.Initial: 50 mg daily in morning or evening throughout menstrual cycle; or, 50 mg daily in morning or evening during luteal phase of menstrual cycle only. Dosage increased each menstrual cycle in 50-mg increments up to 150 mg daily, or each luteal phase up to 100 mg daily, as needed. Once 100-mg daily dosage established for luteal phase, each successive cycle requires a 50-mg titration step for 3 days at the beginning of each luteal phase. Maximum: 150 mg daily for dosing throughout menstrual cycle, or 100 mg daily for dosing during luteal phase only. Route Onset Peak Duration P.O. 2–4 wk* Unknown Unknown

Mechanism of Action

Inhibits reuptake of the neurotransmitter serotonin by CNS neurons, thereby increasing the amount of serotonin available in nerve synapses. An elevated serotonin level may result in elevated mood and reduced depression. This action may also relieve symptoms of other psychiatric conditions attributed to serotonin deficiency.

Contraindications

Concurrent use of disulfiram (oral concentrate) or pimozide; hypersensitivity to sertraline or its components; use within 14 days of an MAO inhibitor

Interactions

aspirin, NSAIDs,
warfarin: Increased anticoagulant activity and risk of bleeding astemizole, terfenadine: Possibly increased blood levels of these , leading to increased risk of arrhythmias
cimetidine: Increased sertraline half-life
MAO inhibitors: Possibly hyperpyretic episodes, hypertensive crisis, serotonin syndrome, and severe seizures moclobemide, serotonergics: Increased risk of potentially fatal serotonin syndrome serotonin and norepinephrine reuptake inhibitors: Increased risk of bleeding, especially GI bleeding tolbutamide: Possibly hypoglycemia tricyclic antidepressants: Possibly impaired metabolism of tricyclic antidepressants, resulting in increased risk of toxicity

Side Efect

CNS: Aggressiveness, agitation, anxiety, dizziness, drowsiness, fatigue, fever, headache, hyperkinesia, insomnia, nervousness, neuroleptic malignant syndrome–like reaction, paresthesia, serotonin syndrome, suicidal ideation, tremor, weakness, yawning
CV: Palpitations
EENT: Dry mouth, epistaxis, sinusitis, vision changes
ENDO: Syndrome of inappropriate ADH secretion
GI: Abdominal cramps, anorexia, constipation, diarrhea, flatulence, increased appetite, indigestion, nausea, vomiting
GU: Anorgasmia, decreased libido, ejaculation disorders, impotence, urinary incontinence
SKIN: Diaphoresis, flushing, purpura, rash
Other: Weight loss

Cautions

Monitor liver function test results and BUN and serum creatinine levels, as sertraline hydrochloride 934 * For antidepressant and antipanic effects; for antiobsessant effect, longer than 4 wk. appropriate, in patients with hepatic or renal dysfunction.
WARNING Monitor patient closely for evidence of serotonin syndrome, such as agitation, hallucinations, coma, tachycardia, labile blood pressure, hyperthermia, hyperreflexia, incoordination, nausea, vomiting, and diarrhea. Serotonin syndrome in its most severe form can resemble neuroleptic malignant syndrome, which includes hyperthermia, muscle rigidity, autonomic instability, possibly rapid changes in vital signs, and mental status changes. Notify prescriber immediately because serotonin syndrome reactions that resemble neuroleptic malignant syndrome may be life-threatening. Be prepared to provide supportive care.

Monitor patient for hypo-osmolarity of serum and urine and for hyponatremia, which may indicate sertraline-induced syndrome of inappropriate ADH secretion.

Be aware that effective antidepressant therapy can promote development of mania in predisposed people. If mania develops, notify prescriber immediately and expect to withhold sertraline.

Watch closely for suicidal tendencies, especially when therapy starts and dosage changes and especially in children and adolescents.

Monitor patient closely for evidence of GI bleeding, especially if patient takes a drug known to cause it, such as aspirin, an NSAID, a serotonin or norepinephrine reuptake inhibitor, or warfarin.

When theray stops, expect to taper dosage to minimize adverse effects rather than stopping drug abruptly.

PATIENT SAFTY

WARNING Tell patient that sertraline increases the risk of serotonin syndrome and reactions that resemble neuroleptic malignant syndrome, rare but serious complications, when taken with some other . Teach patient to recognize signs and symptoms of serotonin syndrome and neuroleptic malignant syndrome, and advise him to notify prescriber immediately if they occur.

Teach patient to dilute oral concentrate before taking it. Tell him to use supplied dropper to remove prescribed amount and mix it with 4 oz (one-half cup) of water, ginger ale, lemon or lime soda, lemonade, or orange juice. Warn him not to mix oral concentrate with anything else. Explain that it’s normal for mixture to be slightly hazy.

Tell patient to take dose immediately after mixing it.

If patient has latex sensitivity, advise him to use an alternate dispenser because the supplied dropper dispenser contains dry natural rubber.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Warn family or caregiver to watch patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes, and especially if patient is a child or adolescent.

Caution patient not to stop taking drug abruptly. Explain that gradual tapering helps to avoid withdrawal symptoms.

Instruct female patients to notify prescriber if they are or could be pregnant and to discuss benefits and risks of continuing sertraline therapy throughout the pregnancy.

Advise patient to consult prescriber before taking any OTC product, especially aspirin products or NSAIDs.

Category

Chemical class: Polyallylamineepichlorhydrin polymer
Therapeutic class: Antihyperphosphatemic

Pregnancy category: C

Indications

To lower serum phosphate level during end-stage renal disease (RENAGEL)
Adults. 2 capsules (806 mg) t.i.d. if serum phosphorus level is 6 to 7.5 mg/dl; 3 capsules (1,209 mg) t.i.d. if serum phosphorus level is 7.6 to 8.9 mg/dl; or 4 capsules (1,612 mg) t.i.d. if serum phosphorus level is 9 mg/dl or more. Dosage increased or decreased gradually by 1 capsule (403 mg)/ meal, as needed. Maximum: 30 capsules (12.1 g) daily. (RENVELA)
Adults. 1 tablet (800 mg) t.i.d. with meals if serum phosphorus level is 5.5 mg/dl to 7.5 mg/dl; or 2 tablets (1,600 mg) if serum phosphorus level is 7.5 mg/dl or greater. Dosage increased or decreased gradually by 1 tablet (800 mg)/meal at 2-wk intervals, as needed.
DOSAGE ADJUSTMENT For patients being switched from calcium acetate to sevelamer carbonate, 1 tablet of sevelamer (800 mg) can be substituted for every 1 tablet of calcium (667 mg) being taken.

Mechanism of Action

Inhibits phosphate absorption in the intestine by binding dietary phosphate, thereby lowering serum phosphorus level.

Contraindications

Fecal impaction, GI obstruction, hypersensitivity to sevelamer or its components, hypophosphatemia, ileus

Interactions

antiarrhythmics, anticonvulsants, digoxin, levothyroxine, liothyronine, quinolones, tetracyclines, theophylline,
warfarin: Possibly altered absorption of these phosphate salts, phosphorus salts: Neutralized therapeutic effects of sevelamer ciprofloxacin: Decreased ciprofloxacin effectiveness

Side Efect

CNS: Headache, fever
CV: Hypertension, hypotension, thrombosis
EENT: Nasopharyngitis
GI: Abdominal pain, constipation (severe), diarrhea, fecal impaction, flatulence, ileus, indigestion, intestinal obstruction oir perforation, nausea, vomiting
RESP: Bronchitis, dyspnea, increased cough, upper respiratory tract infection
MS: Arthralgia, back or limb pain
SKIN: Pruritus, rash
Other: Infection

Cautions

Give other at least 1 hour before or 3 hours after sevelamer to prevent interaction.

Be aware that severe hypophosphatemia may occur in patient with dysphagia, major GI tract surgery, or severe GI motility disorder (including severe constipation) because drug prevents phosphate absorption.

Monitor blood pressure frequently.

Monitor serum phosphorus level to determine drug’s effectiveness; monitor other serum electrolyte levels, especially bicarbonate and chloride, to detect imbalances.

PATIENT SAFTY

Tell patient to take drug with meals and to swallow capsules or tablets whole with water and not to open, break, or chew them.

Caution patient to take other 1 hour before or 3 hours after sevelamer.

Review symptoms of thrombosis, and advise patient to report them immediately.

Instruct patient to report severe or prolonged constipation to prescriber because additional treatment may be needed to prevent serious complications.

Category

Chemical class: Cyclobutanemethanamine
Therapeutic class: Antiobesity

Pregnancy category: C

Controlled substance schedule: IV

Indications

As adjunct to calorie-controlled diet to manage obesity
Adults. Initial: 10 mg daily, increased to 15 mg daily after 4 wk if weight loss is inadequate. Maximum: 15 mg daily.
DOSAGE ADJUSTMENT Reduction to 5 mg daily may be needed if patient can’t tolerate 10-mg dose. sibutramine hydrochloride monohydrate 936

Mechanism of Action

Inhibits central reuptake of dopamine, norepinephrine, and serotonin, thereby suppressing appetite and lowering food intake, leading to weight loss.

Contraindications

Anorexia nervosa, concurrent use of other centrally acting appetite suppressants, history of cardiovascular disease, hypersensitivity to sibutramine or its components, use within 14 days of MAO inhibitor therapy

Interactions

certain decongestants and cough, cold, and allergy ; ephedrine; phenylpropanolamine; pseudoephedrine: Increased risk of elevated blood pressure or heart rate certain opioid analgesics (dextromethorphan, fentanyl, meperidine, pentazocine), dihydroergotamine, lithium, MAO inhibitors, serotonergics, sumatriptan, tryptophan, zolmitriptan: Increased risk of serotonin syndrome erythromycin,
ketoconazole: Possibly decreased sibutramine clearance

Side Efect

CNS: Abnormal dreams, amnesia, anger, anxiety, confusion, depression, dizziness, drowsiness, gait dysfunction, Gilles de la Tourette’s syndrome, headache, hypesthesia, impaired concentration, increased intraocular pressure, insomnia, mania, mood changes, neuroleptic malignant syndrome, nervousness, nightmares, paresthesia, psychosis, serotonin syndrome, short term memory loss, somnolence, speech disorder, stroke, suicidal ideation, transient ischemic attack, tremor, twitching, vertigo
CV: Chest pain, edema, hypertension, MI, palpitations, tachycardia
EENT: Blurred vision, dry eyes or mouth, earache, epistaxis, nasal congestion, rhinitis, sinusitis, taste perversion
GI: Abdominal pain, anorexia, constipation, diarrhea, gastritis, increased appetite, indigestion, nausea, thirst, vomiting
GU: Decreased or increased libido, dysmenorrhea, impotence, urinary frequency, urine retention, UTI, vaginal candidiasis
HEME: Bleeding
MS: Arthralgia, back or neck pain, myalgia, tenosynovitis
SKIN: Acne, alopecia, dermatitis, diaphoresis, ecchymosis, flushing, photosensitivity, urticaria
Other: Anaphylaxis, angioedema, flulike symptoms

Cautions

Administer sibutramine cautiously in patients with mild to moderate renal impairment, and expect to not use it in patients with severe renal impairment, including those with end-stage renal disease receiving hemodialysis.
WARNING Use drug cautiously in patients with a history of substance abuse, and watch for signs of misuse.

Measure blood pressure and pulse rate before and during sibutramine therapy. Notify prescriber about sustained increases, and expect drug to be discontinued

Because serotonin release from nerve terminals has been linked to cardiac valve dysfunction, assess for development of third heart sound.
WARNING If patient takes for migraine, notify prescriber immediately if evidence of serotonin syndrome develops: agitation, anxiety, ataxia, chills, confusion, diaphoresis, disorientation, dysarthria, emesis, excitement, hemiballismus, hyperreflexia, hyperthermia, hypomania, lack of coordination, loss of consciousness, mydriasis, myoclonus, restlessness, tachycardia, tremor, and weakness.

Because drug decreases salivary flow, monitor patient for adverse dental effects.
WARNING Watch closely for evidence of serotonin syndrome, such as agitation, hallucinations, coma, tachycardia, labile blood pressure, hyperthermia, hyperreflexia, incoordination, nausea, vomiting, and diarrhea. In its most severe form, serotonin syndrome can resemble neuroleptic malignant syndrome, which includes hyperthermia, muscle rigidity, autonomic instability, possibly rapid changes in vital signs, and mental status changes. Notify prescriber immediately because serotonin syndrome reactions that resemble neuroleptic malignant syndrome may be lifethreatening. Be prepared to provide supportive care.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

Monitor patient for weight loss to determine drug effectiveness. Expect to discontinue drug if patient has not lost at least 5% of baseline body weight within the first 6 months of treatment.

PATIENT SAFTY

Caution patient not to take sibutramine more often than prescribed.

Teach patient how to measure his blood pressure and pulse rate during therapy.

Explain that sibutramine is an adjunct to reduced-calorie diet, not a replacement for it.

Advise patient to report unusual bleeding or bruising.

Caution against taking OTC products that contain ephedrine because of the increased risk of hypertension.

Urge patient to avoid potentially hazardous activities until drug’s CNS effects are known.

If patient reports dry mouth, suggest sugar-free hard candy or gum or a saliva substitute.
WARNING Tell patient to report any sudden, severe, or persistent symptoms at once.

Urge caregivers to monitor patient closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes and to report concerns immediately to prescriber.

Category

Chemical class: Pyrazolopyrimidinone derivative
Therapeutic class: Antihypertensive (pulmonary arterial), anti-impotence

Pregnancy category: B

Indications

To treat erectile dysfunction
Adults. 50 mg daily, taken 1 hr before sexual activity; increased as prescribed, based on clinical response. Maximum: 100 mg daily.
DOSAGE ADJUSTMENT Initially 25 mg for elderly patients, those with hepatic cirrhosis or creatinine clearance less than 30 ml/min/ 1.73 m2, and those taking potent cytochrome P-450 3A4 inhibitors or ritonavir. Dosage reduced to 25 mg if taken within 4 hr of an alpha blocker. Maximum: 25 mg/ 48 hr. To treat pulmonary arterial hypertension in order to improve exercise ability and delay clinical worsening of condition in patients classified as group 1 by the World Health Organization
Adults. 20 mg t.i.d.
I.V.INJECTION
Adults.10 mg administered as bolus t.i.d. Route Onset Peak Duration P.O. In 30 min Unknown 4 hr

Mechanism of Action

Enhances the effect of nitric oxide released in the penis by stimulation. Nitric oxide increases cGMP level, relaxes smooth muscle, and increases blood flow to the corpus cavernosum, thus producing an erection.

Contraindications

Continuous or intermittent nitrate therapy, hypersensitivity to sildenafil or components

Interactions

barbiturates, bosentan, carabamazepine, efavirenza, nevirapine, phenytoin, rifabutin,
rifampin: Altered plasma level of either drug cimetidine, erythromycin, itraconazole, ketoconazole, mibefradil: Prolonged sildenafil effect doxazosin and other alpha-blockers: Increased risk of symptomatic hypotension nitrates: Profound hypotension protease inhibitors: Increased sildenafil effect
rifampin: Decreased sildenafil effect high-fat meals: Drug absorption delayed by up to 60 minutes

Side Efect

CNS: Cerebrovascular, intracerebral, or subarachnoid hemorrhage; dizziness; headache; migraine; seizures; syncope; transient global amnesia, transient ischemic attack
CV: Heart failure, hypertension, hypotension, myocardial infarction or ischemia, orthostatic hypotension, palpitations, sudden cardiac death, tachycardia, ventricular arrhythmias
EENT: Blurred vision; change in color perception; diplopia; epistaxis; hearing loss; increased intraocular pressure; nasal congestion; nonarteritic anterior ischemic optic neuropathy; ocular burning, pressure, redness or swelling; paramacular edema; photophobia; retinal vascular bleeding or disease; tinnitus, visual decrease or temporary vision loss; vitreous detachment
ENDO: Uncontrolled diabetes mellitus
GI: Diarrhea, indigestion
GU: Cystitis, dysuria, painful erection, priapism, UTI
MS: Arthralgia, back pain
RESP: Pulmonary hemorrhage, upper respiratory tract infection
SKIN: Flushing, photosensitivity

Cautions

Use sildenafil cautiously in patients with renal or hepatic dysfunction, elderly patients, and men with penile abnormalities that may predispose them to priapism.

Also use cautiously in patients with left ventricular outflow obstruction, such as aortic stenosis and idiopathic hypertrophic subaortic stenosis, and those with severely impaired autonomic control of blood pressure because these conditions increase patient’s sensitivity to vasodilators such as sildenafil.

Monitor patient’s blood pressure and heart rate and rhythm before and often during therapy.

Monitor vision, especially in patients over age 50; who have diabetes, hypertension, coronary artery disease, or hyperlipidemia; or who smoke because sildenafil rarely may cause nonarteritic anterior ischemic optic neuropathy that may lead to decreased vision or permanent vision loss.

PATIENT SAFTY

Explain that sildenafil used to treat erectile dysfunction may be taken up to 4 hours before sexual activity but that taking it 1 hour beforehand provides the most effective results.
WARNING Warn patient not to take sildenafil if he also takes any form of organic nitrate, either continuously or intermittently, because profound hypotension and death could result. Also caution patient taking sildenafil for erectile dysfunction not to take more than 25 mg within 4 hours of an alpha blocker, such as doxazosin, because symptomatic orthostatic hypotension can occur.

Tell patient to stop taking drug and contact prescriber if vision decreases suddenly in one or both eyes or if he has a loss of hearing, possibly with tinnitus and dizziness.

Advise patient taking sildenafil for erectile dysfunction to seek sexual counseling to enhance the drug’s effects.

To avoid possible penile damage and permanent loss of erectile function, urge patient to notify prescriber immediately if erection is painful or lasts longer than 4 hours.

Instruct diabetic patient to monitor his blood glucose level frequently because drug may affect glucose control.

Category

Chemical class: Highly selective alpha1adrenergic receptor blocker
Therapeutic class: Benign prostatic antihyperplasia agent

Pregnancy category: B

Indications

To treat symptomatic benign prostatic hyperplasia Adult men. 8 mg daily. Maximum: 8 mg daily.
DOSAGE ADJUSTMENT For patients with moderate renal impairment (creatinine clearance between 30 and 50 ml/min), dosage reduced to 4 mg daily.

Mechanism of Action

Binds to postsynaptic alpha1adrenoreceptors located in the prostate gland, bladder base and neck, and prostatic capsule and urethra. Blocking action at these adrenoreceptor sites causes relaxation of smooth muscle in the local area, which improves urine flow and reduces other benign prostatic hyperplasia symptoms.

Contraindications

Hypersensitivity to silodosin and its components, severe hepatic insufficiency (Child-Pugh score 10 or above), severe renal insufficiency (creatinine clearance less than 30 ml/min/1.73 m2), use with strong CYP3A4 inhibitors such as clarithromycin, ketoconazole, itraconazole, and ritonavir

Interactions

alpha blockers: Possibly increased effects and risk of

Side Efect

antihypertensives: Increased risk of dizziness and orthostatic hypotension cyclosporin, CYP3A4 inhibitors such as clarithromycin, diltiazem, erythromycin, itraconazole, ketoconazole, ritonavir: Possibly increased serum silodosin levels and risk of

Side Efect

Side Efect

CNS: Asthenia, dizziness, headache, insomnia, syncope
CV: Orthostatic hypotension
EENT: Nasal congestion, nasopharyngitis, rhinorrhea, sinusitis
GI: Abdominal pain, diarrhea, elevated liver enzymes,impaired hepatic function,jaundice
GU: Elevated prostate specific antigen level, retrograde ejaculation
SKIN: Purpura, toxic skin eruption

Cautions

Use cautiously in patients with mild renal impairment and mild or moderate hepatic impairment. Patients with moderate renal impairment need
DOSAGE ADJUSTMENT.

Monitor patient’s blood pressure for reduction, especially if he takes an antihypertensive with silodosin.

PATIENT SAFTY

Instruct patient to take drug with a meal.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient planning cataract surgery or other ocular procedure to tell ophthalmologist that he takes silodosin or has taken it in the past because of potential

Side Efect

.

Category

Chemical class: Synthetically derived fermentation product of Aspergillus terreus
Therapeutic class: Antihyperlipidemic

Pregnancy category: X

Indications

To treat hyperlipidemia
Adults. Initial: 20 to 40 mg daily in the evening. Dosage adjusted at 4-wk intervals, as needed, to achieve target LDL-cholesterol level. Maintenance: 5 to 80 mg daily. Maximum: 80 mg daily. To treat homozygous familial hypercholesterolemia
Adults. 40 mg daily in the evening, or 80 mg/day in 3 divided doses—20 mg, 20 mg, and 40 mg (in the evening). Dosage adjusted every 4 wk, as needed, to achieve target LDL-cholesterol level. Maintenance: 5 to 40 mg/day. Maximum: 80 mg daily.
DOSAGE ADJUSTMENT Patients taking cyclosporine or who have severe renal insufficiency should initially receive 5 mg simvastatin daily and be increased as needed to no more than 10 mg daily. Maximum dosage of 10 mg daily should also not be exceeded in patients who are also taking fibrates or niacin. To treat adolescent heterozygous familial hypercholesterolemia Children ages 10 to 17 at least 1 year postmenarche. Initial: 10 mg daily in the evening. Adjusted every 4 wk, as needed, to achieve target LDL-cholesterol level. Maintenance: 10 to 40 mg daily. Maximum: 40 mg daily.
DOSAGE ADJUSTMENT For patients who take cyclosporine, initial dosage reduced to 5 mg/day and maximum dosage reduced to 10 mg/day. For elderly patients and those with renal impairment, initial dosage reduced to 5 mg daily. For patients who take danazol, fibric-acid derivative lipidlowering , such as gemfibrozil, or lipid-lowering doses of niacin (1 g daily or more), maximum dosage reduced to 10 mg daily. For patients who take amiodarone or verapamil, maximum dosage shouldn’t exceed 20 mg daily.

Mechanism of Action

Interferes with the hepatic enzyme hydroxymethylglutaryl-coenzyme A reductase. This action reduces the formation of mevalonic acid, a cholesterol precursor, thus interrupting the pathway necessary for cholesterol synthesis. When the cholesterol level declines in hepatic cells, LDLs are consumed, which in turn reduces the levels of circulating total cholesterol and serum triglycerides. Route Onset Peak Duration P.O. 2 wk 4–6 wk Unknown

Contraindications

Active hepatic disease; breast-feeding; concurrent use with clarithromycin, erythromycin, more than 1 quart of grapefruit juice daily, HIV protease inhibitors, itraconazole, ketoconazole, nefazodone, or telithromycin; hypersensitivity to simvastatin or its components; pregnancy

Interactions

amiodarone, antiretroviral protease inhibitors (amprenavir, indinavir, nelfinavir, ritonavir, saquinavir), clarithromycin, cyclosporine, danazol, gemfibrozil and other fibrates, itraconazole, ketoconazole, erythromycin, nefazodone, niacin (1 g daily or more), telithromycin, verapamil: Increased risk of myopathy or rhabdomyolysis azole antifungals, cyclosporine, gemfibrozil, immunosuppressants, macrolide antibiotics (including erythromycin), niacin, verapamil: Increased risk of acute renal failure bile acid sequestrants, cholestyramine, colestipol: Decreased simvastatin bioavailability digoxin: Possibly slight elevation in blood digoxin level diltiazem, verapamil: Possibly increased blood simvastatin level, increased risk of myopathy oral anticoagulants: Increased bleeding or prolonged PT grapefruit juice (1 or more quarts daily): Possibly increased blood simvastatin level

Side Efect

CNS: Asthenia, dizziness, fatigue, headache
CV: Chest pain
EENT: Cataracts, rhinitis
GI: Abdominal pain, constipation, diarrhea, elevated liver function test results, flatulence, heartburn, hepatic failure, indigestion, nausea, pancreatitis, vomiting
MS: Myalgia, myopathy, rhabdomyolysis
RESP: Upper respiratory tract infection
SKIN: Eczema, pruritus, rash

Cautions

Use simvastatin cautiously in elderly patients and those with renal or hepatic impairment.

Give drug 1 hour before or 4 hours after giving bile acid sequestrant, cholestyramine, or colestipol.

Expect to monitor liver function test results every 3 to 6 months for abnormal elevations.

Monitor serum lipoprotein level, as ordered, to evaluate response to therapy.

PATIENT SAFTY

Urge patient to take drug in the evening.

Urge patient to follow low-fat, cholesterollowering diet.

Urge patient to notify prescriber immediately about muscle pain, tenderness, or weakness and other symptoms of myopathy.

Inform female patient of childbearing age of need to use reliable contraceptive method while taking drug. Instruct her to notify prescriber at once if she suspects pregnancy.

Advise patient to avoid grapefruit juice to decrease risk of drug toxicity.

Category

Chemical class: Macrocyclic lactone
Therapeutic class: Immunosuppressant

Pregnancy category: C

Indications

To prevent rejection of kidney transplantation

ORALL

Adults and adolescents over age 13 weighing 40 kg (88 lb) or more. Initial: 6-mg loading dose. Maintenance: 2 mg daily. Adolescents over age 13 weighing less than 40 kg. Initial: 3-mg/m2loading dose. Maintenance: 1 mg/m2daily.
DOSAGE ADJUSTMENT Maintenance dosage reduced by one-third for patients with impaired hepatic function. Maintenance dosage increased by as much as 400% for patients discontinuing concomitant cyclosporine therapy in order to maintain blood sirolimus trough level of 12 to 24 nanograms/ml. Route Onset Peak Duration P.O. Unknown Unknown Up to 6 mo after discontinuation

Mechanism of Action

Inhibits activation and proliferation of T lymphocytes and antibody production. Sirolimus also inhibits cell cycle progression from the G1 to the S phase, possibly by inhibiting a key regulatory kinase believed to suppress cytokine-driven T-cell proliferation.

Contraindications

Hypersensitivity to sirolimus or its components, malignancy

Interactions

aminoglycosides, amphotericin B, cyclosporine: Possibly impaired renal function bromocriptine, cimetidine, cisapride, clarithromycin, clotrimazole, cyclosporine, danazol, diltiazem, erythromycin, fluconazole, indinavir, itraconazole, ketoconazole, metoclopramide, nicardipine, ritonavir, troleandomycin, verapamil: Possibly increased blood sirolimus level and toxicity calcineurin inhibitors, corticosteroids: Increased risk of deteriorating renal function, serum lipid abnormalities, and UTI carbamazepine, phenobarbital, phenytoin, rifabutin, rifapentine,
St. John’s wort: Possibly decreased blood sirolimus level HMG-CoA reductase inhibitors: Increased risk of rhabdomyolysis when administered concurrently with sirolimus and cyclosporine
rifampin: Significantly increased sirolimus clearance vaccines (killed virus): Possibly decreased immune response to vaccines vaccines (live virus): Increased risk of contracting disease from live virus grapefruit juice: Possibly decreased metabolism of sirolimus high-fat diet: Reduced rate of sirolimus absorption

Side Efect

CNS: Asthenia, fever, headache, insomnia, tremor
CV: Atrial fibrillation, chest pain, hyperlipidemia, hypersensitivity vasculitis, hypertension, pericardial effusion, peripheral edema
ENDO: Hyperglycemia
GI: Abdominal pain, constipation, diarrhea, elevated liver enzymes, hepatotoxicity, nausea, vomiting
GU: Azoospermia, BK viral nephritis, elevated serum creatinine level, nephrotic syndrome, proteinuria, UTI
HEME: Anemia, lymphoma, neutropenia, pancytopenia, thrombocytopenia
MS: Arthralgia, low back or flank pain, joint abnormality
RESP: Dyspnea on exertion, interstitial lung disease, pleural effusion, pulmonary hemorrhage
SKIN: Acne, exfoliative dermatitis, rash
Other: Anaphylaxis; angioedema; delayed wound healing; hypercholesterolemia; hypokalemia; hypophosphatemia; increased susceptibility to infection, including opportunistic infections such as tuberculosis and activation of latent viral infections; lymphedema; weight gain or loss

Cautions

Be aware that sirolimus isn’t recommended in liver or lung transplant patients.

Use sirolimus cautiously in patients who are receiving other known to adversely affect renal function, such as aminoglycosides and amphotericin B; together, they may further decrease renal function.

Monitor patients with existing or recent (including recent exposure to) chickenpox and patients with herpes zoster for worsening symptoms because they have an increased risk of developing severe generalized disease while taking sirolimus.

Mix oral sirolimus with at least 2 oz (60 ml) of water or orange juice in a glass or plastic container. Don’t dilute drug in grapefruit juice or any other liquid.

Stir well and have patient drink solution immediately. Then rinse glass with at least 4 oz (120 ml) of additional liquid, stir well, and have patient drink that liquid to make sure that all of drug is taken.

Give initial dose as soon after transplantation as possible and daily dose 4 hours after cyclosporine, as prescribed.

Monitor whole blood sirolimus concentrations, as ordered, in patients receiving concentrated form of drug, patients weighing less than 40 kg (88 lb), patients with hepatic impairment, and those receiving potent CYP3A4 inducers or inhibitors concurrently.

When using trough level to determine drug’s effectiveness, keep in mind that
DOSAGE ADJUSTMENT should be made only after other factors are taken into account, such as signs, symptoms, and tissue biopsy findings. Keep in mind that interpretation methods vary among laboratories and values aren’t interchangeable.

Monitor serum creatinine level, as ordered, because BK virus associated nephropathy has occurred with sirolimus therapy. In addition, patients receiving sirolimus and cyclosporine may develop impaired renal function. Notify prescriber of any increases in serum creatinine level because sirolimus or cyclosporine dosage may need to be adjusted or drug discontinued.

Monitor patient for urinary protein excretion, as ordered. If protein appears in urine, sirolimus may be discontinued.

Monitor patient for signs and symptoms of infection and check CBC results, as ordered, to detect sirolimus-induced blood dyscrasias or changes in neutrophil count, which may indicate infection.

For patients with hyperlipidemia, be prepared to institute dietary changes, an exercise program, or a lipid-lowering drug regimen if blood cholesterol or triglyceride levels increase because drug may aggravate hyperlipidemia.

PATIENT SAFTY

Advise patient to take sirolimus consistently either with or without food (but not food high in fat) to prevent changes in absorption rate.

Instruct patient to take daily dose with at least 2 oz (60 ml) of water or orange juice. Caution him not to dilute drug in grapefruit juice or any other liquid. Advise him to stir mixture well and drink immediately, then to add at least another 4 oz (120 ml) of liquid to empty container, stir mixture again, and drink that liquid to ensure that he has swallowed all of drug.

Urge patient to avoid people with colds, flu, or other infections because immunosuppression makes him more vulnerable.

Instruct patient not to take live vaccines, such as measles, mumps, rubella, oral polio, bacille Calmette-Guérin, yellow fever, varicella, and TY21a typhoid, during sirolimus therapy.

Advise patient to keep follow-up appointments for blood tests, as ordered.

Category

Chemical class: Beta amino acid derivative
Therapeutic class: Antidiabetic

Pregnancy category: C

Indications

To achieve control of glucose level in type 2 diabetes mellitus as monotherapy or with metformin or other thiazolidinediones
Adults. 100 mg once daily.
DOSAGE ADJUSTMENT For patients with moderate renal insufficiency (creatinine clearance 30 to 50 ml/min/1.73 m2), dosage reduced to 50 mg once daily; for patients with severe renal insufficiency (creatinine clearance less than 30 ml/min/1.73 m2) or end-stage renal disease requiring hemodialysis or peritoneal dialysis, dosage reduced to 25 mg once daily. Route Onset Peak Duration P.O. Unknown 1–4 hr Unknown

Mechanism of Action

Inhibits the dipeptidyl peptidase-4 enzyme to slow inactivation of incretin hormones. These hormones are released by the intestine throughout the day but increase in response to a meal. When blood glucose level is normal or increased, incretin hormones increase insulin synthesis and release from pancreatic beta cells. One type of incretin hormone, glucagon-like peptide (GLP-1) also lowers glucagon secretion from pancreatic alpha cells which reduces hepatic glucose production. These combined actions decrease blood glucose level in type 2 diabetes.

Contraindications

Diabetic ketoacidosis, hypersensitivity to sitagliptin or its components, type 1 diabetes

Interactions

ACE inhibitors, disopyramide, fibric acid derivatives, fluoxetine, sulfonylureas: Possibly increased hypoglycemic effects
beta blockers: Possibly prolonged hypoglycemia or promotion of hyperglycemia digoxin: Slightly increased plasma digoxin level estrogens, oral contraceptives, phenytoin, progestines, thiazide diuretics, triamterene: Possibly decreased hypoglycemic effects

Side Efect

CNS: Headache
EENT: Nasopharyngitis
GI: Abdominal pain, acute pancreatitis, diarrhea, elevated hepatic enzymes, nausea, vomiting
RESP: Upper respiratory tract infection
SKIN: Cutaneous vasculitis, rash, StevensJohnson syndrome, urticaria
Other: Anaphylaxis, angioedema

Cautions

Assess patient’s renal function before starting sitagliptin therapy, as ordered, and periodically thereafter. In moderate to severe renal dysfunction, dosage will be reduced.

Monitor patient for hypersensitivity reactions that, although uncommon, may be severe. If present, notify prescriber and expect sitagliptin to be discontinued.

Monitor patient’s blood glucose level, as ordered, to determine effectiveness of sitagliptin therapy.

PATIENT SAFTY

Stress the need to follow an exercise program and a diet control program during sitagliptin therapy.

Advise patient to notify prescriber immediately if she has trouble breathing, hives, rash, or swelling.

Inform patient that periodic blood tests will be done to determine effectiveness of drug and assess kidney function.

Teach patient how to monitor blood glucose level and when to report changes.

Caution patient that taking other in addition to sitagliptin to control his diabetes may lead to hypoglycemia. Review signs, symptoms, and appropriate prescribed treatment with him.

Instruct patient to contact prescriber if he develops other illnesses, such as infection, or experiences trauma or surgery because his diabetes medication may need adjustment.

Advise patient to carry identification indicating that she has diabetes.

Instruct patient to stop taking sitagliptin and report persistent severe abdominal pain, possibly radiating to the back and accompanied by vomiting.

Category

Chemical class: Electrolyte
Therapeutic class: Antacid, electrolyte replenisher, systemic and urinary alkalizer

Pregnancy category: C

Indications

To treat hyperacidity EFFERVESCENT POWDER Adults and adolescents. 3.9 to 10 g in a glass of water after meals. Maximum: 19.5 g daily. Children ages 6 to 12. 1 to 1.9 g in a glass of water after meals. ORAL POWDER Adults and adolescents. One-half tsp in a glass of water every 2 hr, p.r.n. Maximum: 4 tsp daily in patients up to age 60. Adults and adolescents. 325 mg to 2 g daily to q.i.d., p.r.n. Maximum: 16 g daily. Children ages 6 to 12. 520 mg, repeated once after 30 min, p.r.n. To provide urinary alkalization ORAL POWDER Adults and adolescents. 1 tsp in a glass of water every 4 hr. Maximum: 4 tsp daily in patients up to age 60. Adults and adolescents. Initial: 4 g, then 1 to 2 g every 4 hr. Maximum: 16 g daily. Children. 23 to 230 mg/kg daily, adjusted p.r.n.
IV: Adults and children. 2 to 5 mEq/kg over 4 to 8 hr. To treat metabolic acidosis during cardiac arrest
I.V.INJECTION Adults and children. Initial: 1 mEq/kg, followed by 0.5 mEq/kg every 10 min while arrest continues. To treat less urgent forms of metabolic acidosis
IV: Adults and children. 2 to 5 mEq/kg over 4 to 8 hr.
DOSAGE ADJUSTMENT Dosage reduction possible for elderly patients because of agerelated renal impairment.

Mechanism of Action

Increases plasma bicarbonate level, buffers excess hydrogen ions, and raises blood pH, thereby reversing metabolic acidosis. Sodium bicarbonate also increases the excretion of free bicarbonate ions in urine, raising urine pH; increased alkalinity of urine may help to dissolve uric acid calculi. In addition, it relieves symptoms of hyperacidity by neutralizing or buffering existing stomach acid, thereby increasing the pH of stomach contents.

Incompatibilities

Don’t admix I.V. form of sodium bicarbonate in same solution or administer through same I.V. line as other because precipitate may form.

Contraindications

Hypocalcemia in which alkalosis may lead to tetany; hypochloremic alkalosis secondary to vomiting, diuretics, or nasogastric suction; preexisting metabolic or respiratory alkalosis

Interactions

amphetamines,
quinidine: Decreased urinary excretion of these , possibly resulting in toxicity anticholinergics: Decreased anticholinergic absorption and effectiveness calcium-containing products: Increased risk of milk-alkali syndrome chlorpropamide, lithium, salicylates, tetracyclines: Increased renal excretion and decreased absorption of these ciprofloxacin, norfloxacin, ofloxacin: Decreased solubility of these , leading to crystalluria and nephrotoxicity citrates: Increased risk of systemic alkalosis; increased risk of calcium calculus formation and hypernatremia in patients with history of uric acid calculi digoxin: Possibly elevated digoxin level enteric-coated : Increased risk of gastric or duodenal irritation from rapid removal of enteric coating ephedrine: Increased ephedrine half-life and duration of action H2-receptor antagonists, iron supplements or preparations,
ketoconazole: Decreased absorption of these mecamylamine: Decreased excretion and prolonged effect of mecamylamine methenamine: Decreased methenamine effectiveness
mexiletine: Possibly mexiletine toxicity potassium supplements: Decreased serum potassium level sucralfate: Interference with binding of sucralfate to gastric mucosa urinary acidifiers (ammonium chloride, ascorbic acid, potassium and sodium phosphates): Counteracted effects of urinary acidifiers dairy products: Increased risk of milk-alkali syndrome with prolonged use of sodium bicarbonate

Side Efect

CNS: Mental or mood changes
CV: Irregular heartbeat, peripheral edema (with large doses), weak pulse
EENT: Dry mouth
GI: Abdominal cramps, thirst
MS: Muscle spasms, myalgia
SKIN: Extravasation with necrosis, tissue sloughing, or ulceration

Cautions

Monitor sodium intake of patient taking sodium bicarbonate because effervescent powder contains 700.6 mg of sodium/ 3.9 g; oral powder contains 952 mg of sodium/tsp; and tablets contain 325 mg/ 3.9-mEq tablet, 520 mg/6.2-mEq tablet, and 650 mg/7.7-mEq tablet.

For I.V. infusion, dilute drug with normal saline solution, D5W, or other standard electrolyte solution before administration.

Avoid rapid I.V. infusion, which can cause severe alkalosis. Be aware that during cardiac arrest, risk of death from acidosis may outweigh risks of rapid infusion.

Monitor urine pH, as ordered, to determine drug’s effectiveness as urine alkalizer.

If patient on long-term sodium bicarbonate therapy is consuming calcium or milk, watch for milk-alkali syndrome, characterized by anorexia, confusion, headache, hypercalcemia, metabolic acidosis, nausea, renal insufficiency, and vomiting.

Be aware that parenteral forms are hypertonic and that increased sodium intake can produce edema and weight gain.

Assess I.V. site often for evidence of extravasation. If it occurs, notify prescriber at once and remove I.V. catheter. Elevate the limb, apply warm compresses, and expect prescriber to administer a local injection of hyaluronidase or lidocaine.

PATIENT SAFTY

Advise patient not to take sodium bicarbonate with large amounts of dairy products or for longer than 2 weeks, unless directed by prescriber.

Caution patient not to take more drug than prescribed to avoid

Side Efect

.

Direct patient not to take drug within 2 hours of other oral .

Advise patient to avoid taking other prescribed or OTC without prescriber’s approval because many interact with sodium bicarbonate.

Category

Chemical class: Iron salt, mineral
Therapeutic class: Antianemic

Pregnancy category: B

Indications

To treat iron deficiency anemia in patients receiving long-term hemodialysis and erythropoietin
IV: OR INJECTION
Adults. 125 mg of elemental iron. Usual: Minimum cumulative dose of 1 g elemental iron given over eight sequential dialysis treatments. Dosage repeated at lowest dosage needed to maintain target levels of hemoglobin and hematocrit and acceptable limits of blood iron level.

Mechanism of Action

Acts to replenish iron stores lost during hemodialysis as a result of increased blood loss or increased iron utilization from epoetin therapy. Iron is an essential component of hemoglobin, myoglobin, and several enzymes, including cytochromes, catalase, and peroxidase, and is needed for catecholamine metabolism and normal neutrophil function. Sodium ferric gluconate also normalizes RBC production by binding with hemoglobin or being stored as ferritin in reticuloendothelial cells of the liver, spleen, and bone marrow.

Incompatibilities

Don’t mix sodium ferric gluconate with other or parenteral nutrition solutions for I.V. infusion.

Contraindications

Anemia other than iron deficiency, hypersensitivity to iron salts or their components, iron overload

Interactions

oral iron preparations: Possibly reduced absorption of oral iron supplements

Side Efect

CNS: Asthenia, dizziness, fatigue, fever, headache, hypertonia, nervousness, paresthesia, syncope
CV: Chest pain, generalized edema, hypertension, hypotension, tachycardia
EENT: Dry mouth
GI: Abdominal pain, diarrhea, nausea, vomiting
HEME: Hemorrhage
MS: Back pain, leg cramps
RESP: Cough, dyspnea, upper respiratory tract infection, wheezing
SKIN: Diaphoresis, pruritus
Other: Anaphylaxis, generalized pain, hyperkalemia, hypersensitivity, infusion or injection site reaction

Cautions

To reconstitute sodium ferric gluconate for I.V. infusion, dilute prescribed dosage in 100 ml of normal saline solution immediately before infusion. Infuse over 1 hour. Discard any unused diluted solution.

Inspect drug for particles and discoloration before administration and discard if present.

Give undiluted drug by slow I.V. injection at up to 12.5 mg/min, not to exceed 125 mg per injection.

Be aware that most patients need a minimum cumulative dose of 1 gram of elemental iron administered over eight sequential dialysis treatments.
WARNING Assess patient for evidence of allergic reaction, including chills, facial flushing, pruritus, and rash, and of a hypersensitivity reaction, including diaphoresis, dyspnea, nausea, severe lower back pain, vomiting, and wheezing. Discontinue drug and notify prescriber immediately if patient develops an allergic or hypersensitivity reaction, and be prepared to provide emergency interventions.
WARNING Assess blood pressure often after drug administration because hypotension may occur and may be related to infusion rate or total cumulative dose. Avoid rapid infusion, and be prepared to provide I.V. fluids for volume expansion.

Expect to monitor blood hemoglobin level, hematocrit, serum ferritin level, and transferrin saturation, as ordered, before, during, and after sodium ferric gluconate therapy. Make sure serum iron level is tested 48 hours after last dose. To prevent iron toxicity, notify prescriber and expect to end therapy if blood iron level is normal or elevated.

Assess patient for possible iron overload, characterized by bleeding in GI tract and lungs, decreased activity, pale conjunctivae, and sedation.

PATIENT SAFTY

Warn patient not to take any oral iron preparations during sodium ferric gluconate therapy without first consulting prescriber.

Inform patient that symptoms of iron deficiency may include decreased stamina, learning problems, shortness of breath, and fatigue.

Category

Chemical class: Phenylacetate prodrug
Therapeutic class: Antihyperammonemic

Pregnancy category: C

Indications

As adjunct to treat urea cycle disorders in combination with low-protein diet POWDER, Adults and children weighing more than 20 kg (44 lb). 9.9 to 13 g/m2daily in 4 to 6 divided doses with meals. Children weighing up to 20 kg. 450 to 600 mg/kg daily in 4 to 6 divided doses with meals.

Mechanism of Action

Provides alternate pathway for eliminating waste nitrogen by forming phenylacetate, an active metabolite that conjugates with glutamine to produce phenylacetylglutamine, which is excreted by the kidneys.

Contraindications

Acute hyperammonemia, hypersensitivity to sodium phenylbutyrate or its components

Interactions

corticosteroids: Increased serum ammonia level haloperidol, valproate: Increased risk of hyperammonemia probenecid: Decreased excretion of conjugated product of sodium phenylbutyrate

Side Efect

CNS: Depression, disorientation, fatigue, headache, light-headedness, memory loss, syncope
CV: Arrhythmias
EENT: Hypoacusis, taste perversion
GI: Abdominal pain, anorexia, constipation, elevated liver function test results, gastritis, nausea, peptic ulcer, rectal bleeding, vomiting
GU: Amenorrhea, menstrual irregularities
HEME: Anemia, aplastic anemia, leukocytosis, leukopenia, thrombocytopenia
SKIN: Rash
Other: Body odor, hyperchloremia, hypoalbuminemia, hypophosphatemia, metabolic acidosis, metabolic alkalosis, weight gain

Cautions

Mix powder form of sodium phenylbutyrate with food or liquid, but not with acidic beverages such as coffee and tea.

Be aware that drug shouldn’t be used to treat acute hyperammonemia, which is a medical emergency.

Monitor patient with history of heart failure or severe renal failure for fluid retention because of drug’s sodium content.

PATIENT SAFTY

Instruct patient to take sodium phenylbutyrate with meals but not to mix it with acidic beverages such as coffee and tea.

Advise patient to comply with follow-up laboratory tests, as prescribed.

Urge patient to notify prescriber immediately about changes in body odor because they may signal metabolic imbalance.

Category

Chemical class: Sulfonated cation-exchange resin
Therapeutic class: Antihyperkalemic

Pregnancy category: C

Indications

To treat hyperkalemia ORAL POWDER, SUSPENSION
Adults. 15 g (4 level tsp) once daily to q.i.d. Maximum: 40 g q.i.d. Children. 1 g/kg/dose, as needed. RECTAL POWDER, SUSPENSION
Adults. 25 to 100 g as retention enema, as needed. Children. 1 g/kg/dose as retention enema, as needed. Route Onset Peak Duration P.O. 2–12 hr Unknown Unknown

Mechanism of Action

Releases sodium ions in exchange for other cations in intestines. Resin enters large intestine and releases sodium ions in exchange for hydrogen ions. As the resin moves through the intestines, hydrogen ions are then exchanged for potassium ions, which are in greater concentration. Bound resin leaves the body in feces, carrying potassium and other ions with it, thereby reducing serum potassium level.

Contraindications

Hypersensitivity to sodium polystyrene sulfonate or its components, hypokalemia, obstructive bowel disease, reduced intestinal motility in neonates, oral administration in neonates

Interactions

antacids, laxatives: Increased risk of metabolic alkalosis potassium-sparing diuretics, potassium supplements: Increased risk of fluid retention

Side Efect

CV: Peripheral edema
GI: Abdominal cramps, anorexia, colonic necrosis, constipation, epigastric pain, fecal impaction, GI bleeding, indigestion, ischemic colitis, nausea, perforation, vomiting
GU: Decreased urine output
Other: Hypernatremia, hypocalcemia, hypokalemia, weight gain

Cautions

Use sodium polystyrene sulfonate cautiously in patients with heart failure, hypertension, or marked edema.

Be aware that drug is available as powdered resin or as solution that contains sorbitol to facilitate movement of resin through intestines. As a result, patient may experience abdominal cramps, diarrhea, nausea, and vomiting.

Because the drug doesn’t take effect for sodium polystyrene sulfonate 948 several hours, be aware that it’s inappropriate for treating acute, life-threatening hyperkalemia.

If patient has hypokalemia or hypocalcemia, notify prescriber immediately and expect to withhold drug because it reduces potassium and calcium levels. Evidence of hypokalemia includes abdominal cramps, acidic urine, anorexia, drowsiness, ECG changes, hypotension, hypoventilation, muscle weakness, and tachycardia. Evidence of hypocalcemia includes abdominal pain, agitation, anxiety, ECG changes, hypotension, muscle twitching, psychosis, seizures, and tetany.

To give powdered resin as oral suspension, mix powder in water, syrup, or food and give promptly, being sure to follow full aspiration precautions (such as keeping patient in an upright position while giving drug). If needed, administer through gastric feeding tube.

Precede rectal administration with a cleansing enema, as ordered.

When giving rectally, suspend powdered resin in 100 ml of aqueous solution warmed to body temperature, in bag connected to soft, large (French 28) catheter. Have patient lie on his left side with his lower leg straight and upper leg flexed or with his knees to his chest. Gently insert the tube into the rectum and well into the sigmoid colon. The solution should flow into the colon by way of gravity and be retained for 30 to 60 minutes or longer, if possible. After patient is unable to retain the solution any longer, administer a nonsodium-containing cleansing enema, as prescribed.

Use of sorbitol with sodium polystyrene sulfonate isn’t recommended because of increased risk of colonic necrosis and other serious GI effects, such as bleeding, ischemic colitis, and perforation.

After administration, assess for constipation and fecal impaction.

PATIENT SAFTY

Instruct patient not to mix oral form of sodium polystyrene sulfonate with and liquids high in potassium content, such as bananas and orange juice.

If patient will self-administer rectal solution, teach the correct technique and body position. Remind him to let the solution flow into the colon by gravity and to retain it for at least 30 to 60 minutes, longer if possible.

Advise patient to notify prescriber immediately about abdominal cramps, nausea, and vomiting.

Category

Chemical class: Salicylic acid derivative
Therapeutic class: Analgesic, antiinflammatory

Pregnancy category: Not rated

Indications

To relieve symptoms of acute gout I.V.OR
I.M.INJECTION
Adults. Initial: 100 mg every 3 to 4 hr for 2 days; then 100 mg daily. To relieve pain from musculoskeletal conditions I.V.OR
I.M.INJECTION
Adults. 50 to 100 mg daily or every other day. To relieve symptoms of osteoarthritis I.V.OR
I.M.INJECTION
Adults. 100 mg 3 times/wk for several wk, then once/wk, usually up to a total dosage of 2.5 g. After 1 to 2 wk, another course of treatment may be given. To treat rheumatic fever I.V.OR
I.M.INJECTION
Adults. Initial: 100 to 150 mg every 4 to 8 hr for 3 days, then 100 mg b.i.d.

Mechanism of Action

Exerts peripherally induced analgesic and anti-inflammatory effects by blocking pain impulses and inhibiting prostaglandin synthesis.

Contraindications

GI bleeding; hemophilia; hemorrhage; hypersensitivity to sodium thiosalicylate, NSAIDs, or their components; Reye’s syndrome

Interactions

ACE inhibitors,
beta blockers: Decreased antihypertensive effect of these activated charcoal: Decreased sodium thiosalicylate absorption antacids, urinary alkalizers: Increased excretion of sodium thiosalicylate, leading to reduced drug effectiveness and shortened half-life carbonic anhydrase inhibitors (such as acetazolamide): Increased risk of salicylate toxicity; possibly displacement of acetazolamide from protein-binding sites, resulting in toxicity corticosteroids: Possibly increased sodium thiosalicylate excretion insulin, oral antidiabetic : Altered glucose control (with large sodium thiosalicylate doses) loop diuretics: Possibly decreased effectiveness of loop diuretics in patients with renal or hepatic impairment methotrexate: Increased risk of methotrexate toxicity nizatidine: Increased blood sodium thiosalicylate level probenecid, sulfinpyrazone: Decreased uricosuric effects spironolactone: Possibly inhibited diuretic effect of spironolactone urinary acidifiers (including ammonium chloride, ascorbic acid, methionine): Decreased sodium thiosalicylate excretion, possibly leading to salicylate toxicity
alcohol use: Increased risk of gastrointestinal ulceration

Side Efect

GI: Anorexia, diarrhea, GI bleeding, heartburn, hepatotoxicity, indigestion, nausea, thirst, vomiting
HEME: Leukopenia, platelet dysfunction, prolonged bleeding time, thrombocytopenia
RESP: Bronchospasm
SKIN: Rash, urticaria
Other: Angioedema

Cautions

Use drug cautiously in patients with asthma, chronic urticaria, or nasal polyps because these patients are more prone to hypersensitivity.

Expect to monitor hepatic and renal function during long-term drug therapy.

After repeated use or large doses, look for signs of salicylate toxicity: CNS depression, confusion, diaphoresis, diarrhea, difficulty hearing, dizziness, headache, hyperventilation, lassitude, tinnitus, and vomiting.

Be aware that tinnitus usually means that the blood sodium thiosalicylate level has reached or exceeded the upper limit for therapeutic effects.

PATIENT SAFTY

Instruct patient to notify prescriber immediately about bleeding or symptoms of salicylate toxicity.

Category

Chemical class: Muscarinic receptor antagonist
Therapeutic class: Bladder antispasmodic

Pregnancy category: C

Indications

To treat overactive urinary bladder with symptoms of urge incontinence, urgency, and frequency
Adults. 5 mg daily; if tolerated well, increased to 10 mg daily.
DOSAGE ADJUSTMENT For patients with severe renal impairment or moderate hepatic impairment or patients taking ketoconazole or other potent CYP3A4 inhibitors, dosage limited to 5 mg daily. Route Onset Peak Duration P.O. Unknown 3–8 hr Unknown

Mechanism of Action

Antagonizes the effect of acetylcholine on muscarinic receptors in detrusor muscle, decreasing the muscle spasms that cause inappropriate bladder emptying. This action increases bladder capacity and volume, which relieves the sensation of urgency and frequency and enhances bladder control.

Contraindications

Gastric retention, hypersensitivity to solifesolifenacin succinate 950 nacin or its components, uncontrolled angle-closure glaucoma, urine retention

Interactions

ketoconazole, other potent CYP3A4 inhibitors: Possibly decreased metabolism of solifenacin and increased risk of adverse effects

Side Efect

CNS: Confusion, depression, dizziness, fatigue, hallucinations, headache
CV: Hypertension, prolonged QT interval, peripheral edema, torsades de pointes
EENT: Blurred vision, dry eyes or mouth, pharyngitis
GI: Abdominal pain, constipation, indigestion, nausea, vomiting
GU: UTI, uriney retention
RESP: Cough
RESP: Pruritus, rash, urticaria
Other: Angioedema, influenza

Cautions

Use cautiously in patients with ulcerative colitis, intestinal atony, or myasthenia gravis because solifenacin may decrease GI motility; in patients with significant bladder outflow obstruction because solifenacin may cause urine retention; in patients with hepatic impairment because solifenacin is metabolized in the liver; and in patients with renal impairment because solifenacin excretion may be impaired.

Monitor elderly patients, especially those age 75 and over, for

Side Efect

because they’re at increased risk for solifenacin-induced

Side Efect

.

PATIENT SAFTY

Instruct patient to take solifenacin with a full glass of water and to swallow the tablet whole.

Caution patient to avoid exertion in a warm or hot environment because sweating may be delayed, which could increase body temperature and increase risk of heatstroke.

Advise patient to avoid potentially hazardous activities until drug’s CNS effects are known.

Inform patient that alcohol may cause drowsiness, and urge patient to limit or avoid alcoholic beverages while taking solifenacin.

Category

Chemical class: Recombinant DNA product
Therapeutic class: Growth hormone

Pregnancy category: B

(Serostim) or C (Genotropin, Humatrope, Norditropin, Nutropin, Nutropin AQ, Saizen)

Indications

To treat growth failure caused by growth hormone deficiency SUBCUTANEOUS INJECTION(NUTROPIN, NUTROPIN AQ)
Adults. 0.3 mg (0.9 international units)/ kg/wk. SUBCUTANEOUS INJECTION(SAIZEN)
Adults. Initial: 0.005 mg/kg daily, increased after 4 wk by no more than 0.01 mg/kg daily, as needed. I.M.OR SUBCUTANEOUS INJECTION(HUMATROPE, NUTROPIN, SAIZEN) Children. 0.18 to 0.3 mg (0.54 to 0.9 international units)/kg/wk, divided into equal doses given daily or every other day over 6 to 7 days. SUBCUTANEOUS INJECTION(NORDITROPIN)
Adults. Initial: 0.004 mg/kg daily, increased after 6 wk by no more than 0.016 mg/kg daily, as needed. SUBCUTANEOUS INJECTION(GENOTROPIN, NORDITROPIN) Children. 0.16 to 0.24 mg (0.48 to 0.72 international units)/kg/wk, divided into equal doses given daily over 6 to 7 days. SUBCUTANEOUS INJECTION(TEV-TROPIN) Children. Up to 0.1 mg/kg three times/wk. SUBCUTANEOUS INJECTION(OMNITROPE)
Adults. Initial: 0.04 mg/kg/wk divided into 7 daily doses and increased at 4to 8-wk intervals, as needed. Maximum: 0.08 mg/kg/ wk. Or, 0.15 to 0.30 mg/day. Children. 0.16 to 0.24 mg/kg/wk divided into 6 to 7 daily doses. SUBCUTANEOUS INJECTION(ACCRETROPIN) Children. 0.18 to 0.3 mg/kg/wk divided into 6 to 7 daily doses. To treat growth failure caused by chronic renal insufficiency SUBCUTANEOUS INJECTION(NUTROPIN, NUTROPIN AQ) Children. Up to 0.35 mg (1.05 international units)/kg/wk, divided into equal doses given daily. To treat growth failure caused by Turner’s syndrome SUBCUTANEOUS INJECTION(NUTROPIN, NUTROPIN AQ) Adults and children. Up to 0.375 mg (1.125 international units)/kg/wk, divided into equal doses given daily or every other day over 7 days. SUBCUTANEOUS INJECTION(NORDITROPIN) Adults and children. Up to 0.067 mg/kg/day. SUBCUTANEOUS INJECTION(ACCRETROPIN) Children. 0.36 mg/kg/wk divided into 6 to 7 daily doses. To treat short stature or growth failure in children with short stature homeobox-containing gene (SHOX) deficiency whose epiphyses are not closed SUBCUTANEOUS INJECTION(HUMATROPE) Children. 0.35 mg/kg weekly divided into equal daily doses. To provide long-term treatment of growth failure in children born small for gestational age and no catch-up growth by age 2 SUBCUTANEOUS INJECTION(GENOTROPIN) Children. 0.48 mg/kg/wk, divided into equal doses and administered daily over 6 to 7 days. SUBCUTANEOUS INJECTION(HUMATROPE) Children. Up to 0.47 mg/kg/wk, divided into equal doses and administered daily over 6 to 7 days. SUBCUTANEOUS INJECTION(NORDITROPIN) Children. Up to 0.067 mg/kg/day. To treat growth factor failure due to Prader-Willi syndrome SUBCUTANEOUS INJECTION(GENOTROPIN) Children. 0.24 mg/kg/wk. To treat AIDS-related cachexia or weight loss SUBCUTANEOUS INJECTION(SEROSTIM) Adults weighing more than 55 kg (121 lb). 6 mg at bedtime. Adults weighing 45 to 55 kg (99 to 121 lb). 5 mg at bedtime. Adults weighing 35 to 45 kg (77 to 99 lb). 4 mg at bedtime. Adults weighing less than 35 kg. 0.1 mg/kg at bedtime.
DOSAGE ADJUSTMENT For patients at increased risk for adverse effects related to Serostim, 0.1 mg/kg every other day. For elderly patients, regardless of type of somatropin prescribed, lower starting dose and smaller dosage titration recommended. Route Onset Peak Duration I.M., Unknown Unknown 12–48 hr SubQ

Mechanism of Action

Increases production of somatomedins (or insulin-like growth factor) in the liver and other tissues, which mediates somatropin’s anabolic and growth-promoting effects. The drug binds to specific receptors throughout the body, stimulating amino acid transport; DNA, RNA, and protein synthesis; cell proliferation; and growth of bone and soft tissue. Somatropin also decreases insulin cell receptor sensitivity, thereby increasing blood glucose level; stimulates triglyceride hydrolysis in adipose tissue and hepatic glucose output; and aids bone growth by promoting a positive calcium balance and retention of sodium and potassium.

Contraindications

Active neoplasia; active proliferative or severe nonproliferative diabetic retinopathy; acute critical illness due to complications following open-heart surgery, abdominal surgery, or multiple trauma; acute respiratory failure; cancer; closed epiphyses; hypersensitivity to somatropin, its components, or benzyl alcohol; Prader-Willi syndrome coupled with severe obesity, history of upper airway obstruction or sleep apnea, or severe respiratory impairment

Interactions

anabolic steroids, androgens, estrogens, thyroid hormones: Possibly accelerated epiphyseal closure anticonvulsants, corticosteroids, cyclosporine, sex steroids: Possibly altered clearance of these , increasing risk of adverse effects corticosteroids, corticotropin: Inhibited growth response to somatropin; decreased response of corticosteroids or corticotropin oral estrogens: Decreased somatropin effectiveness

Side Efect

CNS: Depression, dizziness, fatigue, headache, hypoesthesia, insomnia, intracranial hypertension or tumor, paresthesia, weakness
CV: Chest pain, edema, hypertriglyceridemia
EENT: Otitis, papilledema, rhinitis, sinusitis, tonsillitis, vision changes, worsening of diabetic retinopathy
ENDO: Breast pain, edema, tenderness, or mass; gynecomastia; hyperglycemia; hypothyroidism
GI: Nausea, pancreatitis, vomiting
GU: UTI
HEME: Eosinophilia
MS: Arthralgia; back, bone, joint, or leg pain; carpal tunnel syndrome; myalgia; progression of existing scoliosis; slipped capital femoral epiphysis (children)
RESP: Upper respiratory tract infection
SKIN: Increased growth of nevi, rash
Other: Elevated serum alkaline phosphatase, inorganic phosphorus, and parathyroid hormone levels; flulike symptoms; injection site inflammation, lipoatrophy

Cautions

Be aware that somatropin shouldn’t be used in patients with malignancy and should be stopped if patient is diagnosed with malignancy. Cancer treatment must be completed with evidence of remission before somatropin can be started or restarted.

Make sure patient with Prader-Willi syndrome has been evaluated for upper airway obstruction and sleep apnea before starting somatropin because of increased risk of respiratory arrest. Notify prescriber immediately and expect to stop drug if patient starts snoring, snoring increases, or other evidence of upper airway obstruction develops.

Make sure patient has a funduscopic eye examination before starting and periodically throughout somatropin therapy to rule out papilledema.

Use cautiously in elderly patients because they’re more prone to

Side Efect

to somatropin. Expect initial dosage to be lower and
DOSAGE ADJUSTMENT more gradual to minimize adverse effects.

Reconstitute somatropin according to package directions. (Nutropin AQ and forms available in cartridges, such as Norditropin NordiFlex, don’t require reconstitution.) In general, swirl vial gently rather than shaking it to dissolve contents.

Don’t reconstitute with diluent containing benzyl alcohol if drug will be given to neonate. Don’t use diluent supplied for Humatrope for patients sensitive to Metacresol or glycerin; use sterile water for injection.

Store Nutropin AQ vials and cartridges refrigerated in a dark place.

Remember to rotate injection sites to avoid tissue atrophy at injection site.
WARNING Although uncommon, intracranial hypertension is possible. Monitor patient for such signs and symptoms as headache, nausea, papilledema, vision changes, and vomiting, especially during first 8 weeks of therapy. If intrancranial hypertension occurs, notify prescriber, expect to discontinue drug, and provide supportive care, as needed.

Because somatropin is a protein, monitor patient for local or systemic allergic reaction.

Monitor patient’s blood glucose level because somatropin may decrease insulin sensitivity, especially at higher does.

Monitor patient’s thyroid function and obtain periodic test results, as ordered, because untreated hypothyroidsm may interfere with somatropin, especially in children.

Assess patient’s skin regularly for changes that suggest skin malignancy.

PATIENT SAFTY

Instruct diabetic patient who takes insulin to monitor blood glucose level frequently; somatropin may induce insulin resistance.

Inform parents of a child with Turner’s syndrome about increased risk of ear infections.

Advise family or cargiver to observe patient for limping, which may indicate a slipped epiphysis.

Teach patient or caregiver how to measure and administer drug at home using either pen device or vial, syringe, and needle.

Category

Chemical class: Methanesulfonanilide
Therapeutic class: Class III antiarrhythmic

Pregnancy category: B

Indications

To treat life-threatening ventricular arrhythmias
Adults. Initial: 80 mg b.i.d. Maintenance: 160 to 320 mg daily in divided doses b.i.d. or t.i.d. Maximum: 640 mg daily.
DOSAGE ADJUSTMENT If creatinine clearance is 30 to 60 ml/min/1.73 m2, dosage interval extended to every 24 hr; if creatinine clearance is less than 30 ml/min/1.73 m2, dosage interval extended to every 36 to 48 hr, according to response; if creatinine clearance less than 10 ml/min/1.73 m2, dosage adjusted as prescribed. To maintain normal sinus rhythm in patients with highly symptomatic atrial fibrillation who are currently in sinus rhythm
Adults. Initial: If creatinine clearance is 40 to 60 ml/min/1.73 m2, give 80 mg daily; if creatinine clearance exceeds 60 ml/min/ 1.73 m2, give 80 mg b.i.d. Maintenance: After at least 3 days (five or six doses given daily), if 80-mg dose is tolerated and QT interval less than 500 msec, dosage maintained and patient discharged. Or hospitalized patient monitored closely to determine maintenance dosage while increasing to 120 mg b.i.d. for 3 days (five or six doses if daily dosing). Maximum: 160 mg b.i.d. if creatinine clearance exceeds 60 ml/min/ 1.73 m2.
DOSAGE ADJUSTMENT If 80-mg once or twice daily doesn’t reduce frequency of atrial fibrillation relapses and is tolerated without excessive QT-interval prolongation (greater than 520 msec), dosage increased to 120 mg once or twice daily, depending on creatinine clearance. If 120-mg dose doesn’t reduce frequency of early relapse and is tolerated using same criteria, dosage increased to 160 mg once or twice daily, depending on creatinine clearance.
DOSAGE ADJUSTMENT If QT interval is 520 msec or more, dosage reduced until it returns to less than 520 msec. If QT interval exceeds 520 msec with lowest maintenance dosage of 80 mg, drug stopped. If renal function deteriorates, daily dose reduced by half and given daily. Route Onset Peak Duration P.O. Unknown 2–3 hr Unknown

Mechanism of Action

Combines class II and class III antiarrhythmic activity to increase sinus cycle length. This beta blocker decreases AV nodal conduction and increases AV nodal refractoriness. Suppression of SA node automaticity and AV node conductivity decreases atrial and ventricular ectopy.

Contraindications

Asthma, atrial arrhythmias (if baseline QT interval exceeds 450 msec or creatinine clearance is less than 40 ml/min/1.73 m2), cardiogenic shock, congenital or acquired QT syndromes, COPD, heart failure (unless it results from tachyarrhythmia that’s treatable by sotalol), hypersensitivity to sotalol or its components, secondor third-degree AV block without functioning pacemaker, sinus bradycardia

Interactions

allergen immunotherapy, allergenic extracts for skin testing: Increased risk of serious systemic adverse reaction or anaphylaxis amiodarone: Additive depressant effect on conduction, negative inotropic effect anesthetics (hydrocarbon inhalation): Increased risk of myocardial depression and hypotension antacids: Altered sotalol effectiveness astemizole, class I antiarrhythmics, phenothiazines, terfenadine, tricyclic antidepressants: Prolonged QT interval, life-threatening torsades de pointes beta blockers (other): Additive beta blockade beta2-receptor stimulants: Decreased effectiveness of these calcium channel blockers, clonidine, diazoxide, guanabenz, reserpine and other antihypertensives: Additive antihypertensive effect and, possibly, other beta-blocking effects
cimetidine: Possibly impaired sotalol clearance glucagon: Possibly blunted hyperglycemic response insulin, oral antidiabetic : Impaired glucose control, increased risk of hyperglycemia lidocaine: Decreased lidocaine clearance, increased risk of lidocaine toxicity
MAO inhibitors: Increased risk of significant hypertension neuromuscular blockers: Possibly potentiated and prolonged neuromuscular blockade phenothiazines: Increased blood levels of both propafenone: Increased blood level and halflife of sotalol sympathomimetics, xanthines: Possibly mutual inhibition of therapeutic effects

Side Efect

CNS: Anxiety, depression, dizziness, drowsiness, fatigue, insomnia, lethargy, nervousness, weakness
CV: AV conduction disorders, bradycardia, heart failure, hypotension, peripheral vascular insufficiency
EENT: Nasal congestion
ENDO: Hyperglycemia, hypoglycemia
GI: Abdominal pain, constipation, diarrhea, nausea, vomiting
GU: Sexual dysfunction
MS: Muscle weakness
RESP: Bronchospasm, dyspnea, wheezing

Cautions

Expect to obtain baseline creatinine clearance and QT interval before starting sotalol.

Monitor blood pressure, apical and radial pulses, fluid intake and output, daily weight, respiratory rate, and circulation in limbs before and during sotalol therapy.

If prescriber is stopping amiodarone, be aware that sotalol shouldn’t be started until QT interval has returned to baseline because of possible adverse cardiac effects.

Be aware that stopping sotalol abruptly may cause life-threatening reactions.

Monitor serum electrolyte levels because drug can increase risk of torsades de pointes in patients with electrolyte imbalances, especially hypokalemia or hypomagnesemia.

Assess carefully if patient has diabetes mellitus or thyrotoxicosis because they may mask hypoglycemia and hyperthyroidism.

PATIENT SAFTY

Advise patient to notify prescriber immediately if he has difficulty breathing.

Urge patient to consult prescriber before taking OTC , especially cold remedies, which may decrease sotalol’s effectiveness.

Urge patient to avoid hazardous activities until drug’s CNS effects are known.

Category

Chemical class: Fluoroquinolone
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To treat community-acquired pneumonia caused by Chlamydia pneumoniae, Haemophilus influenzae, H. parainfluenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, or Streptococcus pneumoniae and acute bacterial exacerbations of chronic bronchitis caused by C. pneumoniae, Enterobacter cloacae, H. influenzae, H. parainfluenzae, Klebsiella pneumoniae, M. catarrhalis, Staphylococcus aureus, or S. pneumoniae
Adults. 400 mg on day 1, followed by 200 mg/day for 10 days.
DOSAGE ADJUSTMENT For patients with creatinine clearance less than 50 ml/min/ 1.73 m2, 400 mg on day 1 and then dosing interval extended to 200 mg every 48 hr for 9 days.

Mechanism of Action

Causes bacterial cells to die by inhibiting the enzyme DNA gyrase, which is responsible for unwinding and supercoiling bacterial DNA before it replicates.

Contraindications

History of photosensitivity, hypersensitivity to quinolone derivatives, job or lifestyle that precludes compliance with measures to prevent phototoxicity, prolonged QTc interval or use of that can prolong QTc interval

Interactions

aluminum-, calcium-, or magnesiumcontaining antacids; ferrous sulfate; magnesium-containing laxatives; sucralfate; zinc: Decreased bioavailability of sparfloxacin amiodarone, astemizole, bepridil, cisapride, class IA antiarrhythmics (disopyramide, quinidine, procainamide), class III antiarrhythmics (ibutilide, sotalol), erythromycin, pentamidine, phenothiazines, terfenadine, tricyclic antidepressants, other that can prolong QTc interval: Possibly prolonged QTc interval and torsades de pointes

Side Efect

CNS: Asthenia, cerebral thrombosis, dizziness, drowsiness, headache, insomnia, lightheadedness, nervousness, seizures, somnolence
CV: Cardiopulmonary arrest, embolism, prolonged QTc interval, torsades de pointes, vasodilation
EENT: Laryngeal edema, taste perversion
GI: Abdominal pain, diarrhea, hepatic necrosis or failure, hepatitis, intestinal perforation, nausea, pseudomembranous colitis, vomiting
GU: Acute renal failure, vaginal candidiasis
HEME: Agranulocytosis, hemolytic anemia, pancytopenia, thrombocytopenia
MS: Rhabdomyolisis, tendinitis, tendon rupture
RESP: Interstitial pneumonia, pulmonary edema
SKIN: Photosensitivity, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Acidosis, anaphylaxis, angioedema, squamous cell carcinoma

Cautions

Use sparfloxacin cautiously in patients with known or suspected CNS disorders because of risk of seizures. Institute seizure precautions according to facility policy.

Monitor renal and liver function test results, as appropriate, during prolonged therapy.

Measure QTc interval regularly because sparfloxacin has been found to increase QTc interval and risk of torsades de pointes.

Severe diarrhea may indicate pseudomembranous colitis; give fluid, electrolyte, and protein replacement, as ordered.

PATIENT SAFTY

Urge patient to avoid potentially hazardous activities until sparfloxacin’s CNS effects are known.

Advise patient to notify prescriber at once about aching or throbbing tendon pain.

Instruct patient to wait 4 hours after taking sparfloxacin before taking antacids that contain aluminum, calcium, or magnesium; laxatives that contain magnesium; or vitamins that contain iron or zinc.

Caution patient to avoid exposure to sunlight, bright natural light, and other sources of ultraviolet light during therapy and for 5 days afterward. Urge him to wear sunscreen and protective clothing when outdoors.

Urge patient to notify prescriber at first sign of photosensitivity reaction (blistering, burning or swelling sensation, itching, rash, redness).

Category

Chemical class: Aminocyclitol, aminoglycoside derivative
Therapeutic class: Antibiotic

Pregnancy category: Not rated

Indications

To treat acute endocervical, rectal, and urethral gonorrhea caused by susceptible strains of Neisseria gonorrhoeae
I.M.INJECTION Adults and children weighing 45 kg (99 lb) or more. 2 g as a single dose, repeated as prescribed for adult if reinfection occurs or is strongly suspected. Maximum: 4 g for adults, 2 g for children. spectinomycin hydrochloride 956 Children weighing less than 45 kg (except infants). 40 mg/kg as a single dose.

Mechanism of Action

Binds to negatively charged sites on bacterial outer cell membrane, disrupting cell integrity, and binds to bacterial ribosomal subunits, inhibiting protein synthesis. Both actions lead to bacterial cell death.

Contraindications

Hypersensitivity to spectinomycin or its components

Side Efect

CNS: Dizziness, insomnia
GI: Abdominal cramps, nausea, vomiting
Other: Injection site pain

Cautions

To reconstitute spectinomycin, add 3.2 ml bacteriostatic water for injection (with benzyl alcohol) to each 2-g vial or 6.2 ml of diluent to each 4-g vial. Shake vial vigorously before withdrawing dose.

Administer I.M. injection deep into large muscle mass, preferably upper outer quadrant of gluteal muscle.

PATIENT SAFTY

Tell patient he’ll be tested for syphilis at the start of treatment and 3 months later because spectinomycin treatment may mask or delay syphilis symptoms.

Explain risk factors for sexually transmitted diseases, and teach correct condom use.

Advise patient to encourage sexual partner to be tested for gonorrhea.

Instruct patient to notify prescriber if signs and symptoms persist after a few days.

Category

Chemical class: Aldosterone antagonist
Therapeutic class: Aldosterone antagonist, antihypertensive, diagnostic aid for primary hyperaldosteronism, diuretic

Pregnancy category: Not rated

Indications

To treat edema cause by heart failure, hepatic cirrhosis, or nephrotic syndrome
Adults. Initial: 25 to 200 mg daily in divided doses b.i.d. to q.i.d. for at least 5 days. Maintenance: 75 to 400 mg daily in divided doses b.i.d. to q.i.d. Maximum: 400 mg daily. Children. Initial: 1 to 3 mg/kg daily as a single dose or in divided doses b.i.d. to q.i.d. for at least 2 wk; adjusted, as needed, after 5 days. Maximum: 3 times initial dose. To treat hypertension
Adults. Initial: 50 to 100 mg daily as a single dose or in divided doses b.i.d. to q.i.d. for at least 2 wk; gradually adjusted every 2 wk, as needed, to control blood pressure, up to 200 mg daily. Maximum: 400 mg daily. Children. Initial: 1 to 3 mg/kg daily as a single dose or in divided doses b.i.d. to q.i.d. for at least 2 wk; adjusted, as needed, after 5 days. Maximum: 3 times initial dose. To aid in the diagnosis of primary hyperaldosteronism
Adults. For long test, 400 mg daily in divided doses b.i.d. to q.i.d. for 3 to 4 wk; for short test, 400 mg daily in divided doses b.i.d. to q.i.d. for 4 days. To treat primary hyperaldosteronism
Adults. 100 to 400 mg daily in divided doses b.i.d. to q.i.d. before surgery. Maximum: 400 mg daily.
DOSAGE ADJUSTMENT Long-term maintenance dosage decreased for patients at risk for complications during surgery. To substitute as therapy for diureticinduced hypokalemia
Adults. 25 to 100 mg daily as a single dose or in divided doses b.i.d. to q.i.d. Maximum: 400 mg daily. Route Onset Peak Duration P.O.* Unknown 2–3 days 2–3 days

Contraindications

Acute renal insufficiency, anuria, hyperkalemia, hypersensitivity to spironolactone or its components * For diuretic effect; others unknown.

Interactions

ACE inhibitors, cyclosporine, other potassium-sparing diuretics, potassium-containing , potassium supplements: Increased risk of hyperkalemia digoxin: Possibly increased half-life of digoxin exchange resins (sodium cycle), such as sodium polystyrene sulfonate: Increased risk of hypokalemia and fluid retention heparin, oral anticoagulants: Decreased anticoagulant effect of these hypotension-producing : Possibly potentiated antihypertensive or diuretic effect of spironolactone lithium: Possibly lithium toxicity NSAIDs, sympathomimetics: Decreased antihypertensive effect of spironolactone low-salt milk, salt substitutes: Increased risk of hyperkalemia

Side Efect

CNS: Dizziness, encephalopathy, fatigue, headache
EENT: Increased intraocular pressure, nasal congestion, tinnitus, vision changes
ENDO: Gynecomastia
GI: Abdominal pain, anorexia, constipation, diarrhea, flatulence, nausea, vomiting
GU: Impotence
HEME: Aplastic anemia, neutropenia
RESP: Cough, dyspnea
MS: Arthralgia, back and leg pain, muscle weakness, myalgia
Other: Hyperkalemia

Cautions

Be aware that for children or patients who have trouble swallowing, pharmacist may crush spironolactone tablets, mix with flavored syrup, and dispense as a suspension. It’s stable 1 month when refrigerated.

In diagnosing primary aldosteronism, test is considered positive if patient’s serum potassium level rises when spironolactone is given and falls when it’s discontinued.

Expect to evaluate patient’s serum potassium level 1 week after spiraonolactone therapy begins, after each dosage adjustment, monthly for the first 3 months, quarterly for 1 year, and then every 6 months thereafter or as ordered. Notify prescriber if level exceeds 5 mEq/L or patient’s renal function deteriorates (serum creatinine level exceeding 4 mg/ dl). If patient has severe heart failure, follow closely because hyperkalemia may be fatal in such patients.

Evaluate spironolactone’s effectiveness by assessing blood pressure and edema. Blood vessel Aldosterone Receptor H2O H2O H2O H2O H2O Na+ Na+ Na+ Na+ Na+ Distal convoluted tubule Aldosterone Spironolactone Blood vessel Aldosterone Receptor H2O H2O H2O H2O H2O Na+ Na+ Na+ Na+ Na+ Distal convoluted tubule Aldosterone Spironolactone

Mechanism of Action

Normally, aldosterone attaches to receptors on the walls of distal convoluted tubule cells, causing sodium (Na+) and water (H20) reabsorption in the blood, as shown at left. Spironolactone competes with aldosterone for these receptors, thereby preventing sodium and water reabsorption and causing their excretion through the distal convoluted tubules, as shown below right. Increased urinary excretion of sodium and water reduces blood volume and blood pressure.

Stop drug for several days, as prescribed, before patient undergoes adrenal vein catheterization to measure serum aldosterone level and plasma renin activity.

PATIENT SAFTY

Instruct patient to take spironolactone with meals or milk.

If patient can’t swallow tablets, mention that pharmacist can crush and mix them with a flavored syrup as a suspension.

Teach patient who takes spironolactone for hypertension how to measure his blood pressure. Urge him to monitor it regularly and report pressure greater than 140 mm Hg systolic or 90 mm Hg diastolic to prescriber.

Caution patient that he may experience dizziness during spironolactone therapy if fluid balance is altered.

Category

Chemical class: Purified beta-hemolytic Streptococcus filtrate
Therapeutic class: Thrombolytic

Pregnancy category: C

Indications

To lyse coronary artery thrombi
IV:
Adults. 1,500,000 international units within 60 min of event. INTRACORONARY INFUSION
Adults. 20,000-international unit bolus, followed by 2,000 international units/min for 60 min for total dose of 140,000 international units. To lyse acute arterial thromboembolism or thrombosis, acute pulmonary embolism, or deep vein thrombosis
IV:
Adults. 250,000-international unit bolus over 30 min, followed by 100,000 international units/hr for 24 to 72 hr. To clear an occluded arteriovenous cannula
I.V.INJECTION
Adults. 100,000 to 250,000 international units instilled slowly into each occluded lumen.

Mechanism of Action

Binds to fibrin in thrombus and converts trapped plasminogen to plasmin. Plasmin breaks down fibrin, fibrinogen, and other clotting factors, thereby dissolving the thrombus. Route Onset Peak Duration I.V. Immediate 20–120 4 hr min

Incompatibilities

Don’t mix streptokinase in the same syringe or give through the same I.V. line as other .

Contraindications

Active internal bleeding, AV malformation or aneurysm, bleeding diathesis, history of stroke or intracranial or intraspinal surgery within the previous 2 months, hypersensitivity to streptokinase or its components, intracranial cancer, severe uncontrolled hypertension

Interactions

anticoagulants, enoxaparin, heparin, NSAIDs, platelet aggregation inhibitors: Increased risk of bleeding antifibrinolytics: Antagonized effects of both antihypertensives: Increased risk of severe hypotension, especially when streptokinase is administered rapidly to treat coronary artery occlusion cefamandole, cefoperazone, cefotetan, plicamycin,
valproic acid: Possibly hypoprothrombinemia and increased risk of severe hemorrhage corticosteroids, ethacrynic acid, salicylates: Possibly GI ulceration or bleeding

Side Efect

CNS: Chills, fever
CV: Arrhythmias, hypotension
HEME: Unusual bleeding or bruising

Cautions

Obtain hematocrit, platelet count, APTT, PT, and INR, as ordered, before giving streptokinase.

To prevent foaming, don’t shake drug during reconstitution.

Check requently for bleeding at I.V. site and for blood in urine and stool. Perform neurologic assessment to detect intracranial bleeding.

If serious spontaneous bleeding (not controlled by local pressure) occurs, stop streptokinase infusion immediately and notify prescriber.

Monitor heart rate and rhythm by continuous ECG, as ordered.

Treat fever with acetaminophen, as prescribed, rather than aspirin to reduce the risk of bleeding.

PATIENT SAFTY

Explain to patient that he’ll be on bed rest during streptokinase therapy.

Inform patient that minor bleeding may occur at arterial puncture or surgical sites. Reassure him that appropriate care measures will be taken if bleeding occurs.

Advise patient to wear or carry medical alert identification stating that he takes streptokinase.

Inform patient that if he experiences chest pain within 12 months of therapy, he should notify health care providers that he has received streptokinase because repeated administration within 12 months may be ineffective.

Category

Chemical class: Aminoglycoside
Therapeutic class: Antibiotic

Pregnancy category: D

Indications

To treat gram-negative bacillary bacteremia, meningeal infections, pneumonia, systemic infections, and UTI caused by susceptible strains of Aerobacter aerogenes, Brucella, Calymmatobacterium granulomatis, Enterococcus faecalis, Escherichia coli, Haemophilus ducreyi, H. influenzae, Klebsiella pneumoniae, and Proteus
I.M.INJECTION
Adults. 1 to 2 g daily in divided doses every 6 to 12 hr. Maximum: 2 g daily. Children. 20 to 40 mg/kg daily in divided doses every 6 to 12 hr. As adjunct to treat endocarditis caused by Streptococcus viridans or E. faecalis
I.M.INJECTION
Adults. 1 g b.i.d. for 1 wk (S. viridans) or 2 wk (E. faecalis) with a penicillin. Then, 500 mg b.i.d. for 1 wk (S. viridans) or 4 wk (E. faecalis). As adjunct to treat tuberculosis caused by Mycobacterium tuberculosis
I.M.INJECTION
Adults. 1 g daily with other antibiotics; dosage reduced to 1 g 2 or 3 times/wk, as appropriate and prescribed. Maximum: 2 g daily. Children. 20 mg/kg daily with other antibiotics. Maximum: 1 g daily.
DOSAGE ADJUSTMENT For elderly patients, dosage decreased to 500 to 750 mg daily in combination with other antibiotics. To treat plague caused by Yersinia pestis
I.M.INJECTION
Adults. 2 g daily in 2 equally divided doses for at least 10 days. Children. 30 mg/kg daily in divided doses b.i.d. or t.i.d. for 10 days. To treat tularemia caused by Francisella tularensis
I.M.INJECTION
Adults. 1 to 2 g daily in divided doses for 7 to 14 days.
DOSAGE ADJUSTMENT If creatinine clearance is 50 to 80 ml/min/1.73 m2, dosage reduced to 7.5 mg/kg I.M. every 24 hr; if 10 to 49 ml/min/1.73 m2, 7.5 mg/kg I.M. every 24 to 72 hr; if less than 10 ml/min/1.73 m2, 7.5 mg/kg I.M. every 72 to 96 hr.

Mechanism of Action

Binds to negatively charged sites on the bacteria’s outer cell membrane, disrupting cell integrity. Streptomycin also binds to bacterial ribosomal subunits and inhibits protein synthesis. Both actions lead to bacterial cell death.

Incompatibilities

Don’t mix streptomycin in same solution or administer through same I.V. line as other antibiotics.

Contraindications

Hypersensitivity to streptomycin or other aminoglycosides

Interactions

antimyasthenics: Possibly decreased effect of antimyasthenics on skeletal muscle streptomycin sulfate 960 beta-lactam antibiotics: Inactivation of streptomycin capreomycin, other aminoglycosides: Increased potential for ototoxicity, nephrotoxicity, and neuromuscular blockade indomethacin (I.V.): Decreased renal clearance of streptomycin when given to premature neonates, possibly leading to aminoglycoside toxicity methoxyflurane, polymyxins (parenteral): Increased risk of nephrotoxicity and neuromuscular blockade nephrotoxic and ototoxic : Increased risk of nephrotoxicity and ototoxicity neuromuscular blockers: Increased neuromuscular blockade

Side Efect

CNS: Clumsiness, dizziness, neurotoxicity, paresthesia, peripheral neuropathy, seizures, unsteadiness, vertigo
EENT: Hearing loss, sensation of fullness in ears, tinnitus, vision loss
GI: Anorexia, nausea, thirst, vomiting
GU: Decreased or increased urine output, nephrotoxicity
MS: Muscle twitching
SKIN: Erythema, pruritus, rash, urticaria

Cautions

Use streptomycin cautiously in patients with renal impairment. In severely uremic patients, single dose can produce high blood level of drug for several days; cumulative effects may produce ototoxicity.

Expect prescriber to order baseline renal function studies and to assess cranial nerve VIII function (responsible for hearing) at start of streptomycin therapy to allow for later comparisons.

Monitor serum peak and trough levels, as ordered, to ensure adequate but not toxic drug level.

Be aware that streptomycin should be given only by I.M. injection.

To reconstitute streptomycin, add between 4.2 and 4.5 ml of sodium chloride for injection or sterile water for injection to each 1-g vial to provide a concentration of 200 mg/ml, or add between 3.2 and 3.5 ml of diluent to each 5-g vial to provide a concentration of 250 mg/ml. Alternatively, add 6.5 ml of diluent to each 5-g vial to provide a concentration of 500 mg/ml.

Don’t give more than 500 mg/ml.

Rotate injection sites to prevent sterile abscess formation.

PATIENT SAFTY

Advise patient to refrigerate streptomycin solution at 36° to 46° F (2° to 8° C).

Inform patient that treatment for tuberculosis lasts at least 1 year.

Urge patient to notify prescriber if he has fullness or ringing in ears, hearing loss, or vertigo.

Category

Chemical class: Disulfated disaccharide, aluminum salt
Therapeutic class: Antiulcer

Pregnancy category: B

Indications

To prevent duodenal ulcer Adults and adolescents. 1 g b.i.d. To treat active duodenal ulcer ORAL SUSPENSION Adults and adolescents. 1 g q.i.d. 1 hr before meals and at bedtime for 4 to 8 wk, possibly less. Or, 2 g b.i.d. on empty stomach on waking and at bedtime for 4 to 8 wk, possibly less. Adults and adolescents. 1 g q.i.d. 1 hr before meals and at bedtime for 4 to 8 wk, possibly less.

Mechanism of Action

May react with hydrochloric acid in the stomach to form a complex that buffers acid. The complex adheres electrostatically to proteins on the ulcer’s surface and creates a protective barrier at the ulcer site. Sucralfate also inhibits back-diffusion of hydrogen ions and adsorbs pepsin and bile acids, actions that promote healing of an existing duodenal ulcer and prevent ulcer formation.

Interactions

aluminum-containing (such as antacids, antidiarrheals, buffered aspirin with aluminum, and vaginal douches): Possibly aluminum toxicity in patients with renal failure antacids: Possibly interference with binding of sucralfate to GI mucosa cimetidine, ciprofloxacin, digoxin, norfloxacin, ofloxacin, phenytoin, ranitidine, tetracycline,
theophylline: Decreased bioavailability of these

Side Efect

CNS: Dizziness, drowsiness, light-headedness
EENT: Dry mouth
GI: Constipation, diarrhea, indigestion, nausea, vomiting
MS: Back pain
SKIN: Pruritus, rash, urticaria

Cautions

Use sucralfate cautiously in patients with chronic renal failure because of increased risk of aluminum toxicity.

Administer drug to patient when he has an empty stomach.

PATIENT SAFTY

Instruct patient to take sucralfate on an empty stomach at least 1 hour before meals and at bedtime.

Advise patient not to take antacids within 30 minutes of sucralfate.

Caution patient to check with prescriber before taking another drug within 2 hours of sucralfate.

Category

Chemical class: Sulfonamide
Therapeutic class: Antibiotic, antiprotozoal

Pregnancy category: C

Indications

To treat asymptomatic carriers of meningitis Adults and adolescents. 1 g every 12 hr for 2 days. Children ages 1 to 12. 500 mg every 12 hr for 2 days. Children ages 2 to 12 months.500 mg daily for 2 days. To prevent recurrent rheumatic fever Adults and adolescents. 500 mg daily (for patients weighing less than 30 kg [66 lb]) to 1 g daily (for patients weighing 30 kg or more). To treat inclusive nocardiosis Adults and adolescents. 4 to 8 g daily for at least 6 wk. As adjunct to treat toxoplasmosis in patients with AIDS Adults and adolescents. 1 to 2 g every 6 hr, with 50 to 100 mg daily of pyrimethamine and 10 to 25 mg daily of leucovorin. Children age 2 months and over.50 mg/kg b.i.d. for 12 mo, together with 2 mg/kg daily of pyrimethamine for 2 days, then 1 mg/kg/day of pyrimethamine for 2 to 6 mo, then 1 mg/kg daily of pyrimethamine 3 times/wk for remainder of 12 mo; in addition, 5 mg of leucovorin given 3 times/ wk for 12 mo. Maximum: 6 g daily. To treat toxoplasmosis in pregnant women after week 16 of gestation
Adults. 1 g every 6 hr, together with 25 mg daily of pyrimethamine and 5 to 15 mg daily of leucovorin.

Mechanism of Action

Inhibits para-aminobenzoic acid, a bacterial enzyme responsible for synthesizing folic acid, which susceptible bacteria require for growth. By inactivating bacteria, sulfadiazine prevents or alleviates infection.

Contraindications

Breastfeeding; hypersensitivity to sulfadiazine, its components, or other chemically related , such as sulfonamides; pregnancy at term

Interactions

bone marrow depressants: Increased risk of leukopenic or thrombocytopenic effects cyclosporine: Decreased blood cyclosporine level, increased risk of nephrotoxicity estrogen-containing oral contraceptives: Increased risk of breakthrough bleeding and pregnancy hemolytics: Increased risk of adverse effects hepatotoxic : Increased risk of hepatotoxicity hydantoins, oral anticoagulants, oral antidiabetic : Increased or prolonged effects of these , possibly toxicity indomethacin, probenecid, salicylates: Increased blood level of free sulfadiazine caused by displacement from plasma protein–binding sites methotrexate: Increased risk of leukopenic or thrombocytopenic effects of methotrexate phenylbutazone, sulfinpyrazone: Increased blood sulfadiazine level uricosuric : Potentiated uricosuric action

Side Efect

CNS: Dizziness, fatigue, fever, headache, lethargy, weakness
EENT: Pharyngitis
GI: Anorexia, diarrhea, dysphagia, nausea, vomiting
GU: Crystalluria
HEME: Agranulocytosis, aplastic anemia, hemolytic anemia, leukopenia, thrombocytopenia, unusual bleeding or bruising
MS: Arthralgia, myalgia
SKIN: Blisters, erythema, jaundice, pallor, photosensitivity, pruritus, rash
Other: Drug-induced fever

Cautions

Use sulfadiazine cautiously in patients with blood dyscrasias or megaloblastic anemia from folate deficiency because drug may cause blood dyscrasias; in those with G6PD deficiency because hemolysis may occur; in those with hepatic or renal impairment because of increased risk of toxicity; and in those with porphyria because drug may precipitate an acute attack.

Obtain blood sample for CBC and body tissue or fluid specimen for culture and sensitivity tests, as ordered, before giving drug. Expect first dose to be given before results are available.
WARNING Monitor patient for druginduced fever, which may develop 7 to 10 days after starting sulfadiazine therapy. Signs and symptoms may include abdominal pain, anorexia, ataxia, depression, diarrhea, headache, insomnia, nausea, peripheral neuropathy, tinnitus, and vomiting.

Monitor fluid intake and output during therapy. Altered fluid balance may increase risk of crystalluria.

Frequently monitor blood glucose level, and assess for signs and symptoms of hypoglycemia in patients who take an oral antidiabetic drug. Be prepared to respond if hypoglycemia develops.

PATIENT SAFTY

Instruct patient to take sulfadiazine exactly as prescribed and to complete the full course even if he feels better.

Advise patient to take drug with a full glass of water and to drink plenty of fluids during therapy.

Urge patient to notify prescriber if urine turns reddish brown; this may indicate crystalluria.

Inform patient about possible dizziness, and urge him to avoid potentially hazardous activities until drug’s CNS effects are known.

Advise patient to avoid prolonged exposure to sunlight and to wear sunscreen and protective clothing when outdoors.

Urge patient who takes oral contraceptives to use an additional method of birth control during therapy.

Advise patient who takes an oral antidiabetic drug to check his blood glucose level frequently because of the increased risk of hypoglycemia during therapy.

Category

Chemical class: Sulfonamide
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To treat cystitis and other UTIs caused by Enterobacter species, Escherichia coli, Klebsiella species, Proteus mirabilis, P. vulgaris, or Staphylococcus aureus
Adults. 0.5 to 1 g every 6 to 8 hr. Children age 2 months and over.7.5 to 11.25 mg/kg every 6 hr.
DOSAGE ADJUSTMENT Dosage usually reduced for patients with impaired renal function.

Mechanism of Action

Inhibits para-aminobenzoic acid, a bacterial enzyme responsible for synthesizing folic acid, which susceptible bacteria require for growth. By inactivating bacteria, sulfamethizole prevents or alleviates infection.

Contraindications

Breastfeeding; hypersensitivity to sulfamethizole, its components, or other chemically related , such as sulfonamides; pregnancy at term

Interactions

bone marrow depressants: Increased risk of leukopenic or thrombocytopenic effects cyclosporine: Decreased blood cyclosporine level, increased risk of nephrotoxicity estrogen-containing oral contraceptives: Increased risk of breakthrough bleeding and pregnancy hemolytics: Increased risk of adverse effects hepatotoxic : Increased risk of hepatotoxicity hydantoins, oral anticoagulants, oral antidiabetic : Increased or prolonged effects of these , possibly toxicity indomethacin, probenecid, salicylates: Increased blood level of free sulfamethizole caused by displacement from plasma protein–binding sites methotrexate: Increased risk of leukopenic or thrombocytopenic effects of methotrexate phenylbutazone, sulfinpyrazone: Increased blood sulfamethizole level uricosuric : Potentiated uricosuric action

Side Efect

CNS: Dizziness, fatigue, fever, headache, lethargy, weakness
EENT: Pharyngitis
GI: Anorexia, diarrhea, dysphagia, nausea, vomiting
GU: Crystalluria
HEME: Agranulocytosis, aplastic anemia, hemolytic anemia, leukopenia, thrombocytopenia, unusual bleeding or bruising
MS: Arthralgia, myalgia
SKIN: Blisters, erythema, jaundice, pallor, photosensitivity, pruritus, rash
Other: Drug-induced fever

Cautions

Use sulfamethizole cautiously in patients with blood dyscrasias or megaloblastic anemia from folate deficiency because drug may cause blood dyscrasias; in those with G6PD deficiency because hemolysis may occur; in those with hepatic or renal impairment because of increased risk of toxicity; and in those with porphyria because drug may precipitate an acute attack.

Obtain blood sample for CBC and body tissue or fluid specimen for culture and sensitivity tests, as ordered, before giving drug. Expect first dose to be given before results are available.
WARNING Monitor patient for druginduced fever, which may develop 7 to 10 days after sulfamethizole starts. Signs and symptoms include abdominal pain, anorexia, ataxia, depression, diarrhea, headache, insomnia, nausea, peripheral neuropathy, tinnitus, and vomiting.

Monitor fluid intake and output during therapy. Altered fluid balance may increase risk of crystalluria.

Frequently monitor blood glucose level and assess for signs and symptoms of hypoglycemia in patients who take an oral antidiabetic drug. Be prepared to respond if hypoglycemia develops.

PATIENT SAFTY

Instruct patient to take sulfamethizole exactly as prescribed and to complete the full course even if he feels better.

Advise patient to take drug with a full glass of water and to drink plenty of fluids during therapy.

Urge patient to notify prescriber if urine turns reddish brown; this may indicate crystalluria.

Inform patient about possible dizziness, and urge him to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to avoid prolonged exposure to sunlight and to wear sunscreen and protective clothing when outdoors.

Urge patient who takes oral contraceptives to use an additional method of birth control during therapy.

Advise patient who takes an oral antidiabetic drug to check his blood glucose level frequently because of the increased risk of hypoglycemia during therapy.

Category

Chemical class: Sulfonamide
Therapeutic class: Antibiotic, antiprotozoal

Pregnancy category: C

Indications

To treat chlamydial conjunctivitis; malaria (as adjunct to quinine sulfate and pyrimethamine); toxoplasmosis (as adjunct to pyrimethamine); and UTI, including pyelonephritis and cystitis, caused by susceptible organisms
Adults. Initial: 2 g, followed by 1 g every 8 to 12 hr. Children age 2 months and over. Initial: 50 to 60 mg/kg, then 25 to 30 mg/kg every 12 hr. Maximum: 2 g for initial dose, 75 mg/kg daily for subsequent doses.
DOSAGE ADJUSTMENT Dosage reduction usually needed for patients with impaired renal function. To treat uncomplicated urethritis, cervicitis, and proctitis caused by Chlamydia trachomatis
Adults. 1 g every 12 hr for 10 days.
DOSAGE ADJUSTMENT For patients with creatinine clearance of 10 to 30 ml/min/ 1.73 m2, recommended dose reduced by 50% or dosing interval extended; for creatinine clearance of less than 10 ml/min/ 1.73 m2, recommended dose reduced by 75% or dosing interval extended, as prescribed.

Mechanism of Action

Inhibits para-aminobenzoic acid, a bacterial enzyme responsible for synthesizing folic acid, which susceptible bacteria require for growth. By inactivating bacteria, sulfamethoxazole prevents or alleviates infection.

Contraindications

Breastfeeding; hypersensitivity to sulfamethoxazole, its components, or other chemically related , such as sulfonamides; pregnancy at term

Interactions

bone marrow depressants: Increased risk of leukopenic or thrombocytopenic effects cyclosporine: Decreased blood cyclosporine level, increased risk of nephrotoxicity estrogen-containing oral contraceptives: Increased risk of breakthrough bleeding and pregnancy hemolytics: Increased risk of adverse effects hepatotoxic : Increased risk of hepatotoxicity hydantoins, oral anticoagulants, oral antidiabetic : Increased or prolonged effects of these , possibly toxicity indomethacin, probenecid, salicylates: Increased blood level of free sulfamethoxazole caused by displacement from plasma protein-binding sites methotrexate: Increased risk of leukopenic or thrombocytopenic effects of methotrexate phenylbutazone, sulfinpyrazone: Increased blood sulfamethoxazole level uricosuric : Potentiated uricosuric action

Side Efect

CNS: Dizziness, fatigue, fever, headache, lethargy, weakness
EENT: Pharyngitis
GI: Anorexia, diarrhea, dysphagia, nausea, vomiting
GU: Crystalluria
HEME: Agranulocytosis, aplastic anemia, hemolytic anemia, leukopenia, thrombocytopenia, unusual bleeding or bruising
MS: Arthralgia, myalgia
SKIN: Blisters, erythema, jaundice, pallor, photosensitivity, pruritus, rash
Other: Drug-induced fever

Cautions

Use sulfamethoxazole cautiously in patients with blood dyscrasias or megaloblastic anemia from folate deficiency because drug may cause blood dyscrasias; in those with G6PD deficiency because hemolysis may occur; in those with hepatic or renal impairment because of increased risk of toxicity; and in those with porphyria because drug may precipitate an acute attack.

Obtain blood sample for CBC and body tissue or fluid specimen for culture and sensitivity tests, as ordered, before giving drug. Expect first dose to be given before results are available.
WARNING Monitor patient for druginduced fever, which may develop 7 to 10 days after sulfamethoxazole starts. Signs and symptoms include abdominal pain, anorexia, ataxia, depression, diarrhea, headache, insomnia, nausea, peripheral neuropathy, tinnitus, and vomiting.

Monitor fluid intake and output during therapy. Altered fluid balance may increase risk of crystalluria.

Frequently monitor blood glucose level and assess for signs and symptoms of hypoglycemia in patients who take an oral antidiabetic drug. Be prepared to respond if hypogly-cemia develops.

PATIENT SAFTY

Instruct patient to take sulfamethoxazole exactly as prescribed and to complete the full course even if he feels better.

Advise patient to take drug with a full glass of water and to drink plenty of fluids during therapy.

Urge patient to notify prescriber if urine turns reddish brown; this may indicate crystalluria.

Inform patient about possible dizziness, and urge him to avoid potentially hazardous activities until drug’s CNS effects are known.

Advise patient to avoid prolonged exposure to sunlight and to wear sunscreen and protective clothing when outdoors.

Urge patient who takes oral contraceptives to use an additional method of birth control during therapy.

Advise patient who takes an oral antidiabetic drug to check his blood glucose level frequently because of increased risk of hypoglycemia during therapy.

Category

Chemical class: Salicylate, sulfonamide
Therapeutic class: Anti-inflammatory, antirheumatic, immunomodulator

Pregnancy category: B

Indications

To treat inflammatory bowel diseases, such as ulcerative colitis, and to maintain or prolong remission DELAYED-RELEASE , Adults and adolescents. Initial: 500 to 1,000 mg every 6 to 8 hr. Or 500 mg every 6 to 12 hr to decrease adverse GI reactions. Maintenance: 500 mg every 6 hr. Children over age 6. Initial: 6.7 to 10 mg/kg every 4 hr, 10 to 15 mg/kg every 6 hr, or 13.3 to 20 mg/kg every 8 hr. Maintenance: 7.5 mg/kg every 6 hr. To treat rheumatoid arthritis DELAYED-RELEASE ,
Adults. Initial: 500 to 1,000 mg daily during wk 1, increased by 500 mg daily every wk, as needed, up to 2,000 mg daily in divided doses. If no response after 12 wk, increased to 3,000 mg daily. Maintenance: 1,000 mg every 12 hr. Maximum: 3,000 mg daily. To treat juvenile rheumatoid arthritis in patients who have not responded to salicylates or other NSAIDs DELAYED-RELEASE Children ages 6 to 16. 30 to 50 mg/kg daily in divided doses b.i.d. Maximum: 2 g daily.

Mechanism of Action

As a prodrug of sulfapyridine and 5-aminosalicylic acid (mesalamine), delivers more sulfapyridine and mesalamine to the colon than either metabolite could provide alone. Sulfapyridine provides antibacterial action along the intestinal wall; mesalamine inhibits cyclooxygenase, thereby decreasing the production of arachidonic acid metabolites and reducing colonic inflammation.

Contraindications

Hypersensitivity to salicylates, sulfasalazine, sulfonamides, chemically related , or their components; intestinal or urinary obstruction; porphyria

Interactions

bone marrow depressants: Increased leukopenic and thrombocytopenic effects of both digoxin: Possibly inhibited absorption and decreased blood level of digoxin folic acid (vitamin B9): Decreased folic acid absorption hepatotoxic : Increased risk of hepatotoxicity hydantoins, oral anticoagulants, oral antidiabetic : Increased, prolonged, or toxic effects of these methotrexate, phenylbutazone, sulfinpyrazone: Possibly potentiated effects of these

Side Efect

CNS: Ataxia, chills, depression, fatigue, fever, Guillain-Barré syndrome, headache, insomnia, meningitis, peripheral neuropathy, seizures, vertigo, weakness
CV: Pericarditis, vasculitis
EENT: Hearing loss, orange-yellow tears, pharyngitis, tinnitus
GI: Abdominal pain, anorexia, cirrhosis, diarrhea, elevated liver enzymes, hepatitis, hepatotoxicity, indigestion, jaundice, nausea, pancreatitis, ulcerative colitis exacerbation, vomiting
GU: Crystalluria, decreased ejaculatory volume, male infertility, nephritis, nephrotic syndrome, orange-yellow urine, toxic nephrosis
HEME: Agranulocytosis, aplastic anemia, Heinz body or hemolytic anemia, leukopenia, neutropenia, thrombocytopenia, unusual bleeding or bruising
MS: Arthralgia, rhabdomyolysis
RESP: Cyanosis, idiopathic pulmonary fibrosis, lymphocytic interstitial pneumonitis, pleuritis
SKIN: Alopecia, drug rash with eosinophilia and systemic symptoms (DRESS), erythema multiforme, exfoliative dermatitis, epidermal necrolysis, photosensitivity, pruritus, purpura, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria OTHER: Anaphylaxis, lupus erythematosuslike syndrome, serum sickness syndrome

Cautions

Monitor CBC, liver function test results, and BUN and serum creatinine levels before and periodically during prolonged sulfasalazine therapy.

Be aware that sulfasalazine doses over 4 g or a blood level over 50 mcg/ml increases the risk of adverse and toxic reactions.

Monitor fluid intake and output and urine color, pH, and consistency. Acidic urine may require alkalization to prevent crystalluria.

PATIENT SAFTY

Instruct patient to take sulfasalazine with meals, milk, or an antacid to decrease GI distress, and to swallow tablets whole.

Advise patient to prevent crystalluria by taking drug with a full glass of water and drinking at least 64 oz of fluid per day.

Instruct patient and family to administer drug around the clock.

Inform patient that symptom relief may take 2 to 5 days for ulcerative colitis and 4 to 12 weeks for rheumatoid arthritis.

Alert patient that drug may turn urine and skin orange-yellow.

Advise contact lens wearer to consider wearing glasses during therapy because drug can permanently stain contact lenses yellow.

Instruct patient to avoid prolonged sun exposure and to wear protective clothing and sunscreen when outdoors.

Advise patient to brush with a soft-bristled toothbrush and to use dental floss and toothpicks gently because leukopenic and thrombocytopenic drug effects increase risk of infection and gingival bleeding.

Urge patient to return for laboratory tests and follow-up visits to monitor drug’s effect.

Instruct patient to report sore throat, fever, paleness, skin discoloration, or jaundice. These may be signs of serious adverse effects. Explain that prescriber may order tests to determine their cause and that drug may be discontinued until test results are known.

Category

Chemical class: Pyrazalone derivative
Therapeutic class: Antigout, uricosuric

Pregnancy category: Not rated

Indications

To treat chronic or intermittent gouty arthritis
Adults. Initial: 100 to 200 mg b.i.d., increased by 200 mg daily every 2 to 4 days, if needed. Maintenance: 100 to 200 mg b.i.d. Maximum: 400 mg b.i.d. during wk 1; then 200 to 400 mg b.i.d. until serum urate level is controlled. Route Onset Peak Duration P.O. Unknown Unknown 4–10 hr

Mechanism of Action

Inhibits renal tubular reabsorption of uric acid, thereby increasing uric acid excretion and decreasing serum urate level. Decreased serum urate level prevents urate deposition, tophus formation, and chronic joint changes. It also helps resolve existing urate deposits and eventually reduces the number of gouty arthritis attacks.

Contraindications

Active peptic ulcer disease, blood dyscrasias, hypersensitivity to sulfinpyrazone or its components, symptoms of GI inflammation or ulceration

Interactions

acetaminophen: Increased risk of hepatotoxicity, decreased acetaminophen effects aminosalicylate sodium: Increased blood level and prolonged duration of this drug, possibly leading to toxicity antineoplastics: Increased risk of uric acid nephropathy bismuth subsalicylate and other salicylates: Decreased sulfinpyrazone effects cefamandole, cefoperazone, cefotetan, moxalactam, plicamycin,
valproic acid: Possibly hypoprothrombinemia, increased risk of severe hemorrhage diazoxide, mecamylamine, pyrazinamide: Possibly increased serum uric acid level hydantoins: Increased blood hydantoin level, possibly leading to hydantoin toxicity niacin: Possibly decreased uricosuric effect of sulfinpyrazone nitrofurantoin: Decreased nitrofurantoin effectiveness, possibly nitrofurantoin toxicity NSAIDs, oral anticoagulants, platelet aggregation inhibitors, thrombolytics: Increased risk of bleeding oral antidiabetic : Increased risk of hypoglycemia probenecid: Increased sulfinpyrazone effects
theophylline: Possibly decreased blood theophylline level verapamil: Increased clearance and decreased bioavailability of verapamil
alcohol use: Possibly increased serum uric acid level

Side Efect

CNS: Dizziness
EENT: Tinnitus
GI: Abdominal pain, epigastric discomfort, GI bleeding, indigestion, nausea, vomiting
GU: Dysuria, flank pain, hematuria, renal calculi, renal colic, renal failure
HEME: Agranulocytosis, anemia, aplastic anemia, leukopenia, thrombocytopenia
MS: Arthralgia, gouty arthritis (acute attack)
RESP: Bronchospasm, dyspnea, wheezing
SKIN: Erythema, rash

Cautions

Expect to start with full maintenance dose, as ordered, for patient being switched to sulfinpyrazone from another uricosuric.

Monitor serum uric acid level periodically, as ordered, to evaluate drug effectiveness.

Assess for signs of acute gouty arthritis, especially during first few months of sulfinpyrazone therapy.

PATIENT SAFTY

Instruct patient to take sulfinpyrazone with food, milk, or an antacid to prevent GI distress.

Stress the importance of taking drug every day, even when feeling better, to prevent acute gouty arthritis attacks.

Inform patient that acute gouty arthritis may worsen during initial therapy but should improve as treatment continues. Explain that he may not experience drug’s full therapeutic effect for 6 months.

If an acute gouty arthritis attack occurs, advise patient to seek additional treatment but to continue taking sulfinpyrazone, as prescribed, to help prevent exacerbation.

Advise patient to drink at least 80 oz of fluids per day to decrease the risk of renal calculus formation.

Instruct patient to consult prescriber before taking OTC products that contain aspirin or acetaminophen.

Advise patient to avoid alcohol while taking sulfinpyrazone.

Encourage patient to return for ordered follow-up laboratory tests to check for blood dyscrasias.

Category

Chemical class: Sulfonamide
Therapeutic class: Antibiotic, antiprotozoal

Pregnancy category: C

Indications

To treat nocardiosis; plague; malaria (as adjunct to quinine sulfate and pyrimethamine); and UTI, including pyelonephritis and cystitis, caused by susceptible organisms ORAL SUSPENSION, ORAL SYRUP, Adults and adolescents. Initial: 2 to 4 g daily in divided doses. Maintenance: 4 to 8 g daily in divided doses every 4 to 6 hr. Maximum: 8 g daily. Children over age 2 months.Initial: 75 mg/ kg, followed by 120 to 150 mg/kg daily in divided doses every 4 to 6 hr. Maximum: 6 g daily. To treat uncomplicated cystitis in women ORAL SUSPENSION, ORAL SYRUP,
Adults. 2 g as a single dose. To treat acute or recurrent otitis media in combination with erythromycin in penicillin-allergic patients ORAL SUSPENSION, ORAL SYRUP, Children. 150 mg of sulfisoxazole/kg daily and 50 mg of erythromycin/kg daily in divided doses q.i.d. To treat lymphogranuloma venereum ORAL SUSPENSION, ORAL SYRUP,
Adults. 500 mg every 6 hr for 21 days. To treat uncomplicated urethritis, cervicitis, or proctitis caused by Chlamydia trachomatis ORAL SUSPENSION, ORAL SYRUP,
Adults. 500 mg every 6 hr.
DOSAGE ADJUSTMENT For patients with renal impairment, dosing interval changed to every 8 to 24 hr, as prescribed.

Mechanism of Action

Inhibits para-aminobenzoic acid, a bacterial enzyme responsible for synthesizing folic acid, which susceptible bacteria require for growth. By inactivating bacteria, sulfisoxazole prevents or alleviates infection.

Contraindications

Breast-feeding; hypersensitivity to sulfisoxazole, other chemically related , such as sulfonamides, or their components; pregnancy at term

Interactions

bone marrow depressants, methotrexate: Increased risk of leukopenia or thrombocytopenia cyclosporine: Increased risk of nephrotoxicity diuretics: Increased incidence of thrombocytopenic purpura hemolytics (such as doxapram and methyldopa): Increased risk of toxic reaction hepatotoxic (such as amiodarone): Increased risk of hepatotoxicity hydantoins, oral anticoagulants, oral antidiabetic : Increased or prolonged effects of these , possibly toxicity indomethacin, probenecid, salicylates: Increased blood sulfisoxazole level oral contraceptives: Increased risk of breakthrough bleeding with long-term sulfisoxazole use phenylbutazone, sulfinpyrazone: Risk of increased blood sulfisoxazole level thiopental: Increased anesthetic effect of thiopental tolbutamide: Prolonged half-life of tolbutamide uricosurics: Potentiated uricosuric action

Side Efect

CNS: Dizziness, fatigue, fever, headache, lethargy, weakness
EENT: Pharyngitis
GI: Anorexia, diarrhea, dysphagia, nausea, vomiting
GU: Crystalluria
HEME: Agranulocytosis, aplastic anemia, hemolytic anemia, leukopenia, thrombocytopenia, unusual bleeding or bruising
MS: Arthralgia, myalgia
SKIN: Blisters, erythema, jaundice, pallor, photosensitivity, pruritus, rash
Other: Drug-induced fever

Cautions

Use sulfisoxazole cautiously in patients with blood dyscrasias or megaloblastic anemia from folate deficiency because drug may cause blood dyscrasias; in those with G6PD deficiency because hemolysis may occur; in those with hepatic or renal impairment because of increased risk of toxicity; and in those with porphyria because drug may precipitate acute attack.

Obtain blood sample for CBC and tissue or fluid specimen for culture and sensitivity testing, as ordered, before beginning sulfisoxazole therapy. Expect to give first dose before results are available.
WARNING Expect prescriber to discontinue sulfisoxazole if patient exhibits signs of blood dyscrasias, including fever, jaundice, maculopapular or other rash, pallor, pharyngitis, or purpura.

Monitor CBC often, as appropriate, during treatment for signs of

Side Efect

.

Closely monitor patients with AIDS, who are at increased risk for

Side Efect

.
WARNING Monitor patient for druginduced fever, which may develop 7 to 10 days after sulfisoxazole starts. Signs and symptoms include abdominal pain, anorexia, ataxia, depression, diarrhea, headache, insomnia, nausea, peripheral neuropathy, tinnitus, and vomiting.

Monitor fluid intake and output. Unless contraindicated, provide sufficient fluids to maintain a daily urine output of at least 1,200 ml.

For otitis media caused by Haemophilus influenzae, expect to give drug with erythromycin, as prescribed.

Frequently monitor blood glucose level and assess for signs of hypoglycemia in patients who take oral antidiabetic .

PATIENT SAFTY

Instruct patient to take sulfisoxazole exactly as prescribed and to complete the full course of therapy even if he feels better.

Advise patient to take drug with a full glass of water.

Inform patient that tablet may be chewed or crushed and mixed with liquid to ease swallowing.

Advise patient to shake oral suspension well before use and to measure oral suspension or syrup dose with calibrated device to ensure accuracy.

Inform patient that oral suspension or syrup form of drug may be stored at room temperature.

Advise patient to drink 2 to 3 L of fluid daily to maintain hydration, unless contraindicated.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient who takes an oral antidiabetic to check her blood glucose level often because of the risk of hypoglycemia.

Advise patient to avoid prolonged exposure to sunlight and to use sunscreen and wear protective clothing when outdoors.

Category

Chemical class: Pyrroleacetic acid derivative
Therapeutic class: Antigout, antiinflammatory, antirheumatic

Pregnancy category: Not rated

Indications

To decrease pain and inflammation in ankylosing spondylitis, acute attacks of gout or pseudogout, bursitis, moderately painful arthralgia, osteoarthritis, rheumatoid arthritis, and tendinitis Adults and adolescents over age 14. Initial: 150 to 200 mg b.i.d., adjusted based on patient’s response. Maximum: 200 mg b.i.d. To relieve symptoms of acute gouty arthritis, acute subacromial bursitis, and supraspinatus tendinitis Adults and adolescents over age 14. 200 mg b.i.d. for 7 to 14 days; decreased to lowest effective dosage after satisfactory response occurs.
DOSAGE ADJUSTMENT For elderly patients, dosage reduced to 50% of usual adult dosage, if needed.

Mechanism of Action

May block the activity of cyclooxygenase, an enzyme needed to synthesize prostaglandins, which mediate the inflammatory response and cause local vasodilation, swelling, and pain. By blocking cyclooxygenase and inhibiting prostaglandins, this NSAID reduces inflammatory symptoms and pain. Route Onset Peak Duration P.O. In 1 wk* 2–3 wk* Unknown

Contraindications

Angioedema, asthma, bronchospasm, nasal polyps, rhinitis, or urticaria induced by aspirin, iodides, or other NSAIDs

Interactions

acetaminophen, cyclosporine, gold compounds, nephrotoxic : Increased risk of adverse renal effects antacids: Decreased blood level and effects of sulindac antihypertensives: Risk of decreased antihypertensive effect aspirin, salicylates: Decreased sulindac effects, increased risk of GI hemorrhage bone marrow depressants: Increased risk of leukopenia and thrombocytopenia cefamandole, cefoperazone, cefotetan, colchicine, oral anticoagulants, plicamycin, thrombolytics,
valproic acid: Increased risk of bleeding cimetidine, ranitidine: Increased bioavailability of both digoxin: Increased blood digoxin level and risk of digitalis toxicity dimethyl sulfoxide (DMSO): Decreased sulindac effectiveness, possibly peripheral neuropathy with topical application of DMSO diuretics: Possibly decreased loop diuretic effects and increased thiazide diuretic effects glucocorticoids, other NSAIDs, potassium supplements: Increased risk of adverse GI effects hydantoins: Increased blood hydantoin level and risk of phenytoin toxicity insulin, oral antidiabetic : Increased risk of hypoglycemia lithium: Possibly increased blood level and toxic effects of lithium methotrexate: Decreased methotrexate excretion, possibly leading to toxicity platelet aggregation inhibitors: Increased risk of bleeding, additive effects of these probenecid: Increased blood level and adverse and toxic effects of sulindac
alcohol use: Increased risk of adverse GI effects, including GI bleeding

Side Efect

CNS: Aseptic meningitis, cerebral hemorrhage, chills, drowsiness, fever, headache, ischemic stroke, malaise, nervousness, transient ischemic attack
CV: Deep vein thrombosis, edema, heart failure, hypertension, MI, palpitations, peripheral edema, vasculitis
EENT: Tinnitus
ENDO: Hypoglycemia
GI: Abdominal cramps or pain, anorexia, constipation, diarrhea, esophageal irritation, flatulence, gastritis, gastrointestinal bleeding or ulceration, hepatic failure, hepatitis, hepatotoxicity, indigestion, jaundice, liver failure, nausea, perforation of stomach or intestines, vomiting
GU: Acute renal failure, decreased urine output, interstitial nephritis, nephrotic syndrome, polyuria, proteinuria
HEME: Agranulocytosis, aplastic anemia, leukopenia, pancytopenia
RESP: Bronchial spasm, dyspnea, pulmonary edema, wheezing
SKIN: Diaphoresis, erythema multiforme, exfoliative dermatitis, maculopapular rash, pruritus, purpura, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, facial edema, hypersensitivity syndrome

Cautions

Use sulindac with extreme caution in patients with a history of ulcer disease or GI bleeding because NSAIDs such as sulindac increase risk of GI bleeding and ulceration. Expect to use sulindac for the shortest time possible in these patients.

Be aware that serious GI tract ulceration, bleeding, and perforation may occur without
WARNING symptoms. Elderly patients are at greater risk. To minimize risk, give drug with food. If GI distress occurs, with* For antirheumatic effects; unknown for antigout or anti-inflammatory effects. hold drug and notify prescriber at once.

Use sulindac cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.
WARNING Monitor patient closely for thrombotic events, including MI and stroke, because NSAIDs increase the risk.

If patient has systemic lupus erythematosus and mixed connective tissue disease, monitor him closely because sulindac increases the risk of aseptic meningitis.
WARNING If patient has bone marrow suppression or is receiving antineoplastic drug therapy, monitor laboratory results (including WBC count), and watch for evidence of infection because anti-inflammatory and antipyretic actions of sulindac may mask signs and symptoms, such as fever and pain.

Especially if patient is elderly or taking sulindac long-term, watch for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results because, in rare cases, elevated levels may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.

Watch BUN and serum creatinine levels in elderly patients; those with heart failure, impaired renal function, or hepatic dysfunction; and those taking diuretics or ACE inhibitors; because drug may cause renal failure.

Monitor CBC for decreased hemoglobin and hematocrit because drug may worsen anemia.

Assess patient’s skin routinely for rash or other signs of hypersensitivity reaction because sulindac and other NSAIDs may cause serious skin reactions without warning, even in patients with no history of NSAID hypersensitivity. Stop drug at first sign of reaction, and notify prescriber.
WARNING Monitor patient for adventitious breath sounds and dyspnea; sulindac may cause fluid retention, which may precipitate heart failure in susceptible patients.

Expect patient to undergo audiometric examinations before and periodically during prolonged therapy, as ordered.

Monitor patient for evidence of hypersensitivity syndrome, which could become life-threatening. Report multiple occurring and multi-organ

Side Efect

to prescriber and expect drug to be discontinued. Be prepared to provide emergency supportive care, as ordered.

PATIENT SAFTY

Instruct patient to take sulindac exactly as prescribed. Explain that higher doses don’t increase effectiveness and may increase risk of

Side Efect

.

Advise patient to crush tablet and mix with food, if needed, to aid in swallowing.

Instruct patient to take drug with or immediately after meals to decrease GI distress, to take with a full glass of water, and to remain upright for 20 to 30 minutes after administration to prevent drug from lodging in esophagus and causing esophageal irritation.

Urge patient to notify prescriber immediately of chills, fever, rash, or sweating, which may indicate hypersensitivity.

Advise patient to consult prescriber before using acetaminophen, alcohol, aspirin, other NSAIDs, or any OTC during sulindac therapy.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Explain the need for periodic physical examinations and laboratory tests during prolonged therapy to monitor drug effectiveness.

Inform patient that sulindac may increase the risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.

Tell patient that sulindac also may increase the risk of serious adverse GI reactions; stress the need to seek immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.

Alert patient to the possibility of rare but serious hypersensitivity reactions. Urge him to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity.

Category

Chemical class: Serotonin 5-HT1-receptor agonist
Therapeutic class: Antimigraine

Pregnancy category: C

Indications

To relieve acute migraine attacks, with or without aura, or cluster headaches
Adults. 25 to 100 mg as a single dose as soon as possible after onset of symptoms, repeated every 2 hr, as needed and prescribed. Maximum: 300 mg daily.
DOSAGE ADJUSTMENT For patients with hepatic dysfunction, 50 mg is maximum single dose. SUBCUTANEOUS INJECTION
Adults. Initial: 6 mg, repeated after 1 or 2 hr, if needed. Maximum: 2 (6-mg) injections/24 hr. If migraine symptoms return after initial subcutaneous injection, 50 mg P.O. every 2 hr up to 200 mg daily.
NASAL SPRAY
Adults. 1 or 2 sprays (5 or 10 mg) into one nostril as a single dose or 1 spray (20 mg) into one nostril as a single dose. One additional dose may be taken if another attack occurs after at least 2 hr. Maximum: 40 mg daily. Route Onset Peak Duration P.O. In 30 min 2–4 hr Up to 24 hr SubQ In 10 min 1–2 hr Up to 24 hr Nasal In 15 min Unknown Up to 24 hr

Mechanism of Action

May stimulate 5-HT1receptors, causing selective vasoconstriction of inflamed and dilated cranial blood vessels in carotid circulation, thus decreasing carotid arterial blood flow and relieving acute migraines.

Contraindications

Basilar or hemiplegic migraine, cardiovascular disease, concurrent use of ergotamine-containing , hypersensitivity to sumatriptan or its components, ischemic heart disease, Prinzmetal’s angina, use within 14 days of MAO inhibitor therapy, use within 24 hours of another serotonin 5-HT1receptor agonist

Interactions

antidepressants, lithium: Increased risk of serious adverse effects ergotamine-containing : Possibly additive or prolonged vasoconstrictive effects fluoxetine, fluvoxamine, paroxetine, sertraline: Possibly incoordination, hyperreflexia, and weakness
MAO inhibitors: Risk of decreased sumatriptan clearance, increased risk of serious adverse effects

Side Efect

CNS: Anxiety, atypical sensations, dizziness, drowsiness, fatigue, fever, headache, malaise, sedation, seizures, vertigo, weakness
CV: Arrhythmias; chest heaviness, pain, pressure, or tightness; coronary artery vasospasm; ECG changes; hypertension; hypotension; palpitations
EENT: Abnormal vision; nasal burning (P.O., subcutaneous); jaw or mouth discomfort; nasal irritation (nasal); nose or throat discomfort; photophobia (P.O., subcutaneous); taste perversion (nasal); tongue numbness or soreness
GI: Abdominal discomfort, dysphagia
MS: Jaw discomfort, muscle cramps, myalgia, neck pain or stiffness
SKIN: Dermatitis, diaphoresis, erythema, flushing, pallor, photosensitivity (P.O., subcutaneous), pruritus, rash, urticaria
Other: Injection site burning, pain, and redness

Cautions

Be aware that sumatriptan shouldn’t be given to elderly patients because they’re more likely to have decreased hepatic function, coronary artery disease (CAD), and more pronounced blood pressure increases.

Assess patient for chest pain, and monitor blood pressure in patients with CAD before and for at least 1 hour after sumatriptan administration.

Don’t give sumatriptan within 24 hours of another 5-HT1-receptor agonist, such as naratriptan, rizatriptan, or zolmitriptan.

After nasal administration, rinse tip of bottle with hot water (don’t suction water into bottle) and dry with a clean tissue. Replace cap after cleaning.

Inspect injection solution for particles and discoloration before administering. Discard solution if you detect these changes.

Be aware that drug shouldn’t be administered I.V. because this may precipitate coronary artery vasospasm.

Assess patients with risk factors for CAD for arrhythmias, chest pain, and other signs of heart disease.

For patients with seizure disorder, institute seizure precautions according to facility policy because sumatriptan may lower seizure threshold.

PATIENT SAFTY

Advise patient to use sumatriptan as soon as possible after the onset of migraine symptoms.

Urge patient to contact prescriber and avoid taking sumatriptan if headache symptoms aren’t typical.

Remind patient not to exceed prescribed daily dosage.

Advise patient to swallow tablets whole and drink fluids to disguise unpleasant taste.

Show patient suitable sites for subcutaneous injection, and teach him how to load, administer, and discard autoinjector. Or, explain how to administer drug using needle-free drug delivery system, Sumavel DosePro. (Snap off plastic tip, flip back lever into active position, and press end of device to the skin of abdomen or thigh.)

Instruct patient to administer no more than two subcutaneous doses in 24 hours and not to take a second dose if first dose doesn’t provide significant relief.

Inform patient that he may experience burning, pain, and redness for 10 to 30 minutes after subcutaneous injection. Suggest that he apply ice to relieve pain and redness.

Teach patient how to use nasal form correctly.

To avoid cross-contamination, advise patient not to use the same nasal container for more than one person.

Encourage patient to lie down in a dark, quiet room after taking drug to help relieve migraine.

Instruct patient to seek emergency care for chest, jaw, or neck tightness after drug use because drug may cause coronary artery vasospasm; subsequent doses may require ECG monitoring.

Urge patient to report palpitations or rash to prescriber.

Advise patient to avoid potentially hazardous activities until drug’s CNS effects are known.

Alert patient with seizure disorder that drug may lower seizure threshold.

Encourage yearly ophthalmologic examinations for patients who require prolonged drug therapy.

Category

Chemical class: Monoamine acridine
Therapeutic class: Dementia treatment

Pregnancy category: C

Indications

To treat mild to moderate Alzheimer’stype dementia
Adults. Initial: 10 mg q.i.d. for 4 wk, increased to 20 mg q.i.d. and adjusted every 4 wk as prescribed. Maximum: 160 mg daily in 4 divided doses.

Contraindications

Hypersensitivity to tacrine, other acridine derivatives, or their components; jaundice from previous tacrine use; serum bilirubin level that exceeds 3 mg/dl

Interactions

anticholinergics: Decreased effects of both cholinergics, other
cholinesterase inhibitors: Increased effects of these and tacrine, possibly leading to toxicity
cimetidine: Increased blood tacrine level, possibly leading to toxicity neuromuscular blockers: Prolonged or exaggerated muscle relaxation
NSAIDs: Increased gastric acid secretion, possibly GI irritation and bleeding
theophylline: Increased blood theophylline level, possibly leading to toxicity T T Acetylcholine N receptor M receptor Acetic acid Tacrine Choline Cholinergic neuron Cholinergic synapse Cholinesterases Cholinesterases Acetylcholine Acetylcholine N receptor M receptor Acetic acid Tacrine Choline Cholinergic neuron Cholinergic synapse Cholinesterases Cholinesterases Acetylcholine

Mechanism of Action

Tacrine may relieve dementia in patients with Alzheimer’s disease by increasing the acetylcholine level in the CNS. In Alzheimer’s disease, some cholinergic neurons lose their ability to function, which decreases the acetylcholine level. The remaining functioning cholinergic neurons release acetylcholine, but it’s enzymatically broken down by cholinesterases into acetic acid and choline, as shown below left. Without acetylcholine to activate muscarinic (M) and nicotinic (N) receptors on postsynaptic cell membranes, nerve transmission and excitability decrease. Tacrine binds with and inhibits cholinesterases, making more intact acetylcholine available in cholinergic synapses, as shown below right. This prolongs and enhances acetylcholine’s effects, which increases nerve transmission and reduces symptoms of dementia. all : Reduced tacrine bioavailability smoking: Possibly decreased tacrine effectiveness

Side Efect

CNS: Agitation, anxiety, asthenia, ataxia, confusion, depression, dizziness, fatigue, hallucinations, headache, hostility, insomnia, seizures, somnolence, syncope, tremor
CV: Arrhythmias, chest pain, conduction disturbances, hypertension, hypotension, palpitations, peripheral edema, sick sinus syndrome
EENT: Rhinitis
GI: Abdominal pain, anorexia, constipation, diarrhea, elevated liver function test results, flatulence, indigestion, nausea, vomiting
GU: Bladder obstruction, urinary frequency and incontinence, UTI
MS: Back pain, muscle stiffness, myalgia
RESP: Asthma, cough, upper respiratory tract infection, wheezing
SKIN: Flushing, jaundice, purpura, rash
Other: Weight loss

Cautions

In patients with asthma, monitor for wheezing and increased mucus production because tacrine may increase bronchoconstriction and bronchial secretions.

Expect to monitor hepatic enzyme levels (specifically ALT), as ordered, every other week from at least week 4 to week 16 of tacrine therapy.

If patient has elevated serum ALT level, monitor her for signs and symptoms of hepatitis, such as jaundice and rightupper-quadrant pain. ALT level should return to normal 4 to 6 weeks after therapy stops.

Once ALT level returns to normal, expect to begin tacrine therapy again (starting at 10 mg q.i.d.) as prescribed, and check patient’s hepatic enzyme levels weekly for 16 weeks, monthly for 2 months, and then every 3 months thereafter, as ordered.

Monitor patient for bradyarrhythmias, conduction disturbances, and sick sinus syndrome because tacrine may have a vagotonic effect on the heart rate.
WARNING Be aware that tacrine’s cholinergic effects may exacerbate seizures or parkinsonian symptoms.

Monitor patient’s urine output and assess for abdominal distention and abnormal bowel sounds because drug’s cholinergic effects may exacerbate conditions involving urinary tract or GI obstruction or ileus.

Be aware that patients with peptic ulcer disease and those receiving NSAIDs are at increased risk for developing diarrhea, nausea, and vomiting because tacrine increases gastric acid secretion.

Assess patient for increased signs and symptoms because drug becomes less effective as Alzheimer’s disease progresses and the number of intact cholinergic neurons declines.

PATIENT SAFTY

Instruct patient to take tacrine on an empty stomach, and advise caregiver to make sure that the patient swallows the drug.

If patient experiences GI distress, suggest taking drug with meals. Mention that drug’s effects may be delayed.

Urge patient to seek assistance when walking and changing position until drug’s effects are known. Instruct her to avoid potentially hazardous activities during this period.

Advise patient not to smoke because it decreases drug’s effectiveness.

Caution patient not to stop taking drug abruptly. Doing so may impair cognitive ability.

Inform caregiver that tacrine will become less effective as Alzheimer’s disease progresses.

Urge caregiver to make sure patient returns regularly for follow-up visits and laboratory tests to monitor drug effectiveness.

Category

Chemical class: Macrolide
Therapeutic class: Immunosuppressant

Pregnancy category: C

Indications

To prevent organ rejection in patients undergoing allogeneic liver, kidney, or heart transplantation .Adults having kidney transplantation. 0.2 mg/kg/day given in two equally divided doses every 12 hr beginning only after renal function has recovered (serum creatinine level of 4 mg/dl or less).
DOSAGE ADJUSTMENT Black patients may need higher doses after kidney transplantation. Adults having liver transplantation. 0.10 to 0.15 mg/kg/day given in two equally divided doses every 12 hr. Administer 6 hr after transplantation. Adults having heart transplantation. 0.075 mg/kg/day given in two equally divided doses every 12 hr. Administer 6 hr after transplantation. Children having liver transplantation. 0.15 to 0.20 mg/kg/day given in two equally divided doses every 12 hr. Administer 6 hr after transplantation.
IV: Adults having kidney or liver transplantation. 0.03 to 0.05 mg/kg/day as a continuous infusion beginning no sooner than 6 hr after transplantation. Adults having heart transplantation. 0.0187 to 0.025 mg/kg/day as a continuous infusion beginning no sooner than 6 hr after transplantation. Children having liver transplantation. 0.03 to 0.05 mg/kg/day as a continuous infusion beginning no sooner than 6 hr after transplantation.
DOSAGE ADJUSTMENT Therapy delayed up to 48 hours or longer in patients with postoperative oliguria. For patients with hepatic or renal impairment, dosage kept at lower end of range with possible need for further reduction.

Mechanism of Action

Inhibits T-lymphocyte activation, possibly by binding to an intracellular protein, FKBP-12. This binding results in formation of a complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin, which inhibits phosphatase activity of calcineurin. This inhibition may prevent dephosphorylation and translocation of nuclear factor of activated T-cells, a nuclear component thought to initiate gene transcription for the formation of lymphokines. The result is inhibition of T-lymphocyte activation, which produces immunosuppression.

Incompatibilities

Don’t store diluted drug in PVC containers because of increased instability of tacrolimus and possible extraction of phthalates. Don’t mix or co-infused tacrolimus with solutions of pH 9 or greater, such as with acyclovir or ganciclovir, because of chemical instability of tacrolimus in alkaline media.

Contraindications

Breast-feeding, hypersensitivity to tacrolimus or its components, hypersensitivity to polyoxyl 60 hydrogenated castor oil (parenteral form), ocular exposure, within 24 hours of cyclosporine therapy

Interactions

aminoglycosides, amphotericin B, cisplatin, cyclosporine, other nephrotoxic : Increased risk of renal impairment bromocriptine, chloramphenicol, cimetidine, cisapride, clarithromycin, clotrimazole, cyclosporine, danazol, diltiazem, erythromycin, ethinyl estradiol, fluconazole, ganciclovir, itraconazole, ketoconazole, lansoprazole, magnesium-aluminum-hydroxide, metoclopramide, methylprednisolone, nefazodone, nicardipine, nifedipine, nelfinavir, omeprazole, protease inhibitors, ritonavir, troleandomycin, verapamil, voriconazole: Possibly increased blood tacrolimus level carbamazepine, caspofungin, phenobarbital, phenytoin, rifabutin, rifampin, sirolimus, St. John’s wort: Possibly decreased blood tacrolimus level mycophenolic acid: Possibly increased plasma mycophenolic acid level
phenytoin: Possibly increased blood phenytoin level sirolimus: Increased risk of wound healing complications, renal dysfunction, and insulin-dependent post-transplant diabetes mellitus vaccines (live or killed): Possibly suppressed immune response and increased adverse effects of vaccine grapefruit juice: Possibly increased blood tacrolimus trough levels in liver transplant patients high-fat : Decreased absorption of oral tacrolimus

Side Efect

CNS: Asthenia, fever, dizziness, headache, hemiparesis, insomnia, jittery feeling, leukoencephalopathy, mental changes, mutism, neurotoxicity, paresthesia, posterior reversible encephalopathy syndrome, progressive multifocal leukoencephalopathy, seizures, speech disorder, stroke, syncope, tremor
CV: Atrial and ventricular arrhythmias, cardiac arrest, chest pain, hypercholesterolemia, hyperlipemia, hypertension, hypertriglyceridemia, myocardial hypertrophy or ischemia, MI, pericardial effusion, peripheral edema, QT-interval prolongation, torsades de pointes, venous thrombosis
EENT: Blindness, cortical blindness, deafness, hearing loss, photophobia
ENDO: Cushingoid features, diabetes mellitus, hot flashes, hyperglycemia
GI: Abdominal pain, anorexia, ascites, bile duct stenosis, colitis, constipation, diarrhea, dyspepsia, enterocolitis, gastric ulcer, gastroenteritis, gastroesophageal reflux disease, hepatic impairment or toxicity, impaired gastric emptying, nausea, pancreatitis, venoocclusive liver disease, vomiting
GU: Acute renal failure, BK virus nephropathy, elevated creatinine and BUN levels, hemorrhagic cystitis, hemolytic-uremic syndrome, micturition abnormality, nephrotoxicity, oliguria, renal impairment, UTI
HEME: Anemia, decreased platelet count, disseminated intravascular coagulation, leukocytosis, neutropenia, pancytopenia, thrombocytopenia
MS: Arthralgia, back pain
RESP: Acute respiratory distress syndrome, atelectasis, bronchitis, cough increase, dyspnea, interstitial lung disease, lung infiltration, pleural effusion, respiratory distress or failure
SKIN: Flushing, malignancy, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis, cytomegalovirus infection, hyperkalemia, hypokalemia, hypomagnesemia, hypophosphatemia, impaired wound healing, lymphoproliferative or malignant disorders, multi-organ failure, opportunistic infections (including activation of latent viral infections), primary graft dysfunction, weight loss

Cautions

Don’t start tacrolimus therapy within 24 hours of cyclosporine, and vice versa. If tacrolimus or cyclosporine blood levels are elevated beyond 24 hours of either drug being discontinued, the other drug should not be started until elevation is resolved.

Be aware that I.V. tacrolimus therapy should only be given if patient can’t tolerate oral tacrolimus. Patient should be switched to oral therapy as soon as possible.

Expect to give drug with adrenal corticosteroid therapy.

Dilute intravenous drug with normal saline solution or 5% dextrose to 0.004 to 0.02 mg/ml following manufacturer guidelines. Once diluted, drug should be stored in glass or polyethylene containers (not PVC, because of decreased stability and possible extraction of phthalates). Discard after 24 hours if not used.

When converting patient from parenteral to oral therapy after heart transplantation, expect to give oral form 8 to 12 hours after infusion is discontinued.

Be aware that children having liver transplantation usually need higher doses of tacrolimus than
Adults.
WARNING Closely monitor patient for anaphylaxis at least during first 30 minutes of I.V. administration. Make sure emergency equipment and , such as aqueous solution of epinephrine and oxygen, are immediately available.

Monitor patient’s blood tacrolimus trough levels regularly, as ordered. Higher trough levels increase risk of toxicity.

Monitor blood pressure, especially in patients with history of hypertension, because drug can worsen this condition.

Monitor results of liver and renal function tests, as ordered, to detect signs of decreased function.

Tacrolimus may increase serum cholesterol, lipid, and triglyceride levels.

Monitor patient’s blood glucose level closely because tacrolimus may cause post-transplant diabetes mellitus with the need for insulin therapy, especially in black and Hispanic patients. tacrolimus 978

Monitor patient’s serum potassium level, as ordered, because drug can alter it.

Watch for evidence of neurotoxicity, especially in patients receiving high doses of drug. Evidence of encephalopathy includes headache, impaired consciousness, loss of motor function, psychiatric disturbance, seizures, and tremors.

PATIENT SAFTY

Advise patient to take oral doses 12 hours apart at same time each day.

Instruct patient to take capsules on an empty stomach.

Tell patient to avoid consuming grapefruit juice while taking tacrolimus.

Advise patient not to stop taking drug without consulting prescriber.

Instruct patient not to receive virus vaccines during therapy. Urge him to avoid people who have received such vaccines or to wear a protective mask when he’s around them.

Caution patient to avoid having contact with people who have infections during therapy because tacrolimus causes immunosuppression.

Stress importance of having repeated laboratory tests while taking tacrolimus, and urge compliance.

Inform patient that tacrolimus therapy may result in insulin-dependent diabetes. Tell him to report frequent urination or an increase in thirst, hunger, or fatigue.

Instruct patient to limit exposure to direct sunlight and to wear protective clothing and use sunscreen when exposure can’t be avoided.

Category

Chemical class: Phosphodiesterase inhibitor
Therapeutic class: Anti-impotence

Pregnancy category: B

Indications

To treat erectile dysfunction
Adults. Initial: 10 mg daily taken 1 hr before sexual activity; dosage decreased to 5 mg or increased to 20 mg, as prescribed, based on clinical response. Maximum: 20 mg daily. Or, 2.5 mg once daily, increased to 5 mg once daily, if needed.
DOSAGE ADJUSTMENT For patients taking potent CYP3A4 inhibitors such as itraconazole, ketoconazole, or ritonavir, dosage shouldn’t exceed 10 mg every 72 hr. For patients with moderate to severe renal insufficiency who take drug on an as-needed basis, dosage shouldn’t exceed 5 mg daily. For patients with mild to moderate hepatic impairment who take drug on an as-needed basis, dosage shouldn’t exceed 10 mg daily. For patients who take drug once daily, no
DOSAGE ADJUSTMENT is needed with mild to moderate hepatic or renal impairment; once daily dosing not recommended for use with severe hepatic or renal impairment. To treat pulmonary arterial hypertension in order to improve exercise ability in patients classified as group 1 by the World Health Organization (ADCIRCA)
Adults.40 mg once daily.
DOSAGE ADJUSTMENT For patients with mild to moderate hepatic or renal impairment or who have already taken ritonavir for at least 1 week, initial dosage of 20 mg once daily and then increased as tolerated. For patient already taking tadalafil and being prescribed ritonavir, tadalafil temporarily discontinued for at least 24 hours before ritonavir starts. Then, after at least 1 week of ritonavir, tadalafil restarted at 20 mg once daily and then increased to 40 mg once daily, as tolerated. Route Onset Peak Duration P.O. Unknown 30 min– Unknown 6 hr

Mechanism of Action

Enhances the effect of nitric oxide released in the penis during sexual stimulation. Nitric oxide activates the enzyme guanylate cyclase, which causes increased levels of cGMP in the corpus cavernosum. This leads to increased blood flow to the penis, thus producing an erection.

Contraindications

Continuous or intermittent nitrate therapy, hypersensitivity to tadalafil or its compotadalafil 979 T nents, retinitis pigmentosa

Interactions

carbamazepine, phenytoin, phenobarbitol: Possibly decreased tadalafil effects doxazosin, tamsulosin and other alpha blockers: Increased risk of symptomatic hypotension erythromycin, itraconazole, ketoconazole, ritonavir: Prolonged tadalafil effects nitrates: Profound hypotension protease inhibitors (other than ritonavir): Possibly prolonged tadalafil effects
rifampin: Decreased tadalafil effects grapefruit juice: Possibly prolonged tadalafil effects
alcohol use: Potentiated blood pressure lowering effects

Side Efect

CNS: Asthenia, dizziness, fatigue, headache, hypesthesia, insomnia, migraine, paresthesia, seizures, somnolence, stroke, syncope, transient global amnesia, vertigo
CV: Angina pectoris, chest pain, hypotension, hypertension, MI, postural hypotension, palpitations, sudden cardiac death, tachycardia
EENT: Blurred vision, changes in color vision, conjunctivitis, dry mouth, epistaxis, eyelid swelling, eye pain, hearing loss, increased lacrimation, nasal congestion, nasopharyngitis, nonarteritic anterior ishcemic optic neuropathy, pharyngitis, retinal artery or vein occlusion, visual field defects
GI: Abnormal liver function studies, diarrhea, dysphagia, dyspepsia, esophagitis, gastroesophageal reflux, gastritis, increased gamma-glutamyl transpeptidase levels, nausea, upper abdominal pain, vomiting
GU: Priapism, spontaneous penile erection, UTI
MS: Arthralgia, back or neck pain, extremity pain, myalgia
RESP: Bronchitis, cough, dyspnea, upper respiratory tract infection
SKIN: Diaphoresis, exfoliative dermatitis, flushing, pruritus, rash, Stevens-Johnson syndrome, urticaria
Other: Facial edema, flulike symptoms, hypersensitivity reactions

Cautions

Know that patients with hereditary degenerative retinal disorders, including retinitis pigmentosa, should not receive tadalafil because of the risk of serious ophthalmic

Side Efect

.

Patients with severe hepatic or renal impairment should not receive tadalafil because its effects in these patients are unknown.

Use tadalafil cautiously in patients with left ventricular outflow obstruction, such as aortic stenosis and idiopathic hypertrophic subaortic stenosis, and those with severely impaired autonomic control of blood pressure because these conditions increase sensitivity to vasodilators such as tadalafil.

Use tadalafil cautiously in patients with conditions that may predispose them to priapism, such as sickle cell anemia, multiple myeloma, leukemia, or penile deformities (such as angulation, cavernosal fibrosis, or Peyronie’s disease).

Monitor blood pressure and heart rate and rhythm before and during therapy.

PATIENT SAFTY

Explain that, when used as needed to treat erectile dysfunction, tadalafil should be taken 1 hour before sexual activity to provide the most effective results. Alternatively, if the patient chooses to take a smaller dose of tadalfil daily, encourage him to take it at about the same time every day regardless of the timing of sexual activity.
WARNING Tell patient not to take tadalafil if he takes any form of organic nitrate, either continuously or intermittently, because profound hypotension and death could result. Tell him to seek immediate medical attention if he has a sudden loss of vision or hearing.

If patient takes tadalafil to treat erectile dysfunction, advise him to obtain sexual counseling to help enhance the drug’s effects.

To avoid possible penile damage and permanent loss of erectile function, urge patient to notify prescriber immediately if erection is painful or lasts longer than 4 hours.

Advise patient to limit alcohol consumption while taking tadalafil.

Category

Chemical class: Triphenylethylene derivative
Therapeutic class: Nonsteroidal antiestrogen agent, partial estrogen agonist

Pregnancy category: D

Indications

To treat metastatic breast cancer in men and women; to treat node-negative breast cancer in women, or node-positive breast cancer in postmenopausal women, after total or segmental mastectomy, axillary dissection, and breast irradiation
Adults. 20 to 40 mg daily. Dosages greater than 20 mg administered b.i.d. To reduce the risk of invasive breast cancer in women with ductal carcinoma in situ (DCIS) after surgery and radiation, to reduce the risk of breast cancer in women at high risk
Adults. 20 mg daily for 5 yr.

Mechanism of Action

May block the effects of estrogen on breast tissue by competing with estrogen for estrogen-receptor binding sites. Estrogen may stimulate the growth of cancer cells.

Contraindications

Hypersensitivity to tamoxifen or its components; women at high risk for breast cancer and women with ductal carcinoma in situ and a history of deep vein thrombosis or pulmonary embolus or who need coumarin-type anticoagulant therapy; use with anastrozole therapy

Interactions

bromocriptine: Possibly increased blood tamoxifen level estrogens: Possibly altered therapeutic effect of tamoxifen warfarin and other coumarin-type anticoagulants: Increased anticoagulant effect of these

Side Efect

CNS: Confusion, depression, dizziness, fatigue, headache, light-headedness, somnolence, stroke, weakness
CV: Edema, hyperlipidemia, thrombosis
EENT: Keratopathy, ocular toxicity (including cataracts), optic neuritis, retinopathy
GI: Elevated liver function test results, hepatotoxicity, nausea, vomiting
GU: Endometrial cancer, endometrial hyperplasia, endometrial polyps, genital itching, menstrual irregularities, ovarian cysts, uterine malignancies, vaginal discharge (females); impotence, decreased libido (males)
HEME: Anemia, leukopenia, thrombocytopenia
MS: Transient bone or tumor pain
RESP: Pulmonary embolism
SKIN: Bullous pemphigoid, dry skin, erythema multiforme, rash, Stevens-Johnson syndrome, thinning hair
Other: Angioedema, hot flashes, hypercalcemia, weight gain

Cautions

WARNING Make sure that patient has been informed about serious or potentially lifethreatening adverse effects associated with tamoxifen before therapy begins. Be aware that women with ductal carcinoma in situ and those at high risk for breast cancer are more likely to develop uterine cancer, stroke, or pulmonary emboli than others receiving tamoxifen.

If patient is premenopausal, begin drug therapy in the middle of menstruation; if patient’s menstrual cycles are irregular, verify that she has had a negative pregnancy test before therapy starts.

Expect patient to undergo an ophthalmic examination before and periodically during tamoxifen therapy. Also expect to monitor patient for adverse ocular reactions, such as cataracts.

Assess patient for signs and symptoms of thromboembolic events, such as shortness of breath, leg pain, and change in mental status.

Periodically monitor patient’s platelet and WBC counts, cholesterol and triglyceride levels, and liver function test results, as ordered.

Monitor blood calcium level and assess tamoxifen citrate 981 T patient for signs and symptoms of hypercalcemia, such as nausea, vomiting, and thirst; tamoxifen may cause hypercalcemia in breast cancer patients with bone metastasis within a few weeks of starting treatment.

Store tamoxifen in a closed, light-resistant container at room temperature.

PATIENT SAFTY

Advise patient to swallow tamoxifen tablet whole with water.

Instruct premenopausal patient to use a nonhormonal form of contraception, such as a condom or diaphragm, during tamoxifen therapy. Emphasize that she shouldn’t become pregnant while taking drug and for 2 months afterward. Advise her to notify prescriber at once if she becomes pregnant during therapy.

Inform patient of the most common side effects—hot flashes, vaginal discharge, and irregular menses.

Urge patient to immediately notify prescriber if she notices a rash, itching, difficulty breathing, or facial swelling because they may signify a hypersensitivity reaction.

Advise patient to notify prescriber if she experiences leg pain or calf swelling during tamoxifen therapy because they may indicate a blood clot.

Instruct patient to report signs of hepatotoxicity, such as tiredness, nausea, yellow skin, and flulike symptoms.

Advise patient to have regular gynecologic exmainations and to notoify prescriber about abnormal symptoms, including abdominal or pelvic pain, new breast lumps, and unusual vaginal discharge or bleeding.

Urge patients who take tamoxifen for prophylaxis to have regular mammograms because tamoxifen doesn’t prevent all cancers.

Stress the importance of taking tamoxifen regularly. Urge patient to consult prescriber if

Side Efect

, such as nausea and vomiting, are interfering with dosage schedule. These symptoms may be a sign of hypercalcemia.

Inform women who wish to breast-feed that tamoxifen my appear in breast milk and cause serious adverse effects in the infant.

Category

Chemical class: Sulfamoylphenethylamine derivative
Therapeutic class: Benign prostatic hyperplasia (BPH) treatment

Pregnancy category: B

Indications

To treat BPH
Adults. Initial: 0.4 mg daily 30 min p.c. for 2 to 4 wk, increased to 0.8 mg daily if no response to initial dosage. Maximum: 0.8 mg daily.

Mechanism of Action

Blocks alpha1-adrenergic receptors in the prostate. This action inhibits smoothmuscle contraction in the prostate, prostatic capsule, prostatic urethra, and bladder neck, which improves the rate of urine flow and reduces symptoms of BPH.

Contraindications

Hypersensitivity to tamsulosin, quinazolines, or their components

Interactions

alpha blockers: Additive effects of both
cimetidine: Risk of decreased tamsulosin clearance CYP2D6 inhibitors (such as fluoxetine, paroxetine, terbinafine), CYP3A4 inhibitors (such as erythromycin, ketoconazole): Possibly increased plasma tamsulosin level phosphodiesterase-5 inhibitors: Increased risk of hypotension

Side Efect

CNS: Asthenia, dizziness, drowsiness, headache, insomnia, syncope, vertigo
CV: Chest pain, orthostatic hypotension
EENT: Amblyopia, diplopia, intraoperative floppy iris syndrome, pharyngitis, rhinitis
GI: Diarrhea, nausea
GU: Decreased libido, ejaculation disorders, priapism
MS: Back pain tamsulosin hydrochloride 982
RESP: Respiratory impairment
SKIN: Pruritus, rash, urticaria
Other: Angioedema

Cautions

Be aware that prostate cancer should be ruled out before tamsulosin therapy begins.

Give drug about 30 minutes after the same meal each day.

If patient takes drug on an empty stomach, monitor his blood pressure because of the increased risk of orthostatic hypotension.

If patient doesn’t take drug for several days, resume therapy at 0.4 mg/dose, as prescribed.

PATIENT SAFTY

Instruct patient not to open, crush, or chew tamsulosin capsules and to take drug about 30 minutes after the same meal each day.

Instruct patient to notify prescriber if he misses several days of therapy, and caution him against restarting drug at previous dosage.

Advise patient to avoid potentially hazardous activities until drug’s CNS effects are known. Mention the need for caution if dosage is increased.

Advise patient to change position slowly, especially after initial dose and each dosage increase, to minimize effects of orthostatic hypotension.

Category

Chemical class: Mu-opioid agonist
Therapeutic class: Centrally acting synthetic analgesic

Pregnancy category: C

Controlled substance schedule: II

Indications

To relieve moderate to severe acute pain
Adults. 50 mg to 100 mg repeated every 4 to 6 hr, as needed. Maximum: 700 mg on first day; 600 mg daily thereafter
DOSAGE ADJUSTMENT On first day of therapy, second dose may be given as soon as 1 hour after first dose, if needed. For patients with moderate hepatic impairment (Child-Pugh Class B), dosage should not exceed 50 mg for each episode, and intervals between doses should be at least 8 hours. Route Onset Peak Duration P.O. Unknown 1 hr 4 hr

Mechanism of Action

Binds with and activates opioid receptors (mainly mu receptors) in brain and spinal cord and inhibits norepinephrine reuptake to produce analgesia.

Contraindications

Acute or severe bronchial asthma, hypercapnia or significant respiratory depression not monitored or without available resuscitation equipment, hypersensitivity to tapentadol or its components, paralytic ileus, within 14 days of MAO inhibitor therapy

Interactions

CNS depressants: Increased risk of CNS depression
MAO inhibitors: Possibly hyperpyretic episodes, hypertensive crisis, serotonin syndrome, and severe seizures serotonergics: Increased risk of potentially fatal serotonin syndrome
alcohol use: Increased risk of CNS depression

Side Efect

CNS: Abnormal dreams, anxiety, confusion, dizziness, fatigue, headache, insomnia, lethargy, seizure, serotonin syndrome, somnolence, syncope, tremor
CV: Hypotension
EENT: Dry mouth, nasopharyngitis
ENDO: Hot flash
GI: Constipation, dyspepsia, nausea, vomiting
GU: Anorexia, UTI
MS: Arthralgia
RESP: Respiratory depression, upper respiratory infection
SKIN: Diaphoresis, pruritis, rash, urticaria
Other: Hypersensitivity reactions, physical or psychological dependence, withdrawal

Cautions

Be aware that tapentadol isn’t recommended for patients with severe renal impairment (creatinine clearance less than 30 ml/min/1.73 m2) or severe hepatic dysfunction (Child-Pugh Class C).

Use tapentadol cautiously in patients with hypoxia, hypercapnia, or decreased respiratory reserve such as may occur in asthma, COPD, cor pulmonale, severe obesity, sleep apnea syndrome, myxedema, kyphoscoliosis, CNS depression, or coma. Also use cautiously in patients with head injury or conditions in which increased intracranial pressure may occur because drug may obscure the signs and symptoms. Also use cautiously in patients with mild to moderate renal or hepatic dysfunction and in patients with biliary tract disease, including acute pancreatitis, because drug may cause spasm of the sphincter of Oddi.

Expect to begin tapentadol therapy at lower doses in elderly patients because of age-related decreased renal and hepatic function.

Monitor patient’s respiratory rate, depth, and effort during tapentadol therapy because drug may cause respiratory depression, especially in elderly or debilitated patients and in those who have conditions accompanied by hypoxia, hypercapnia, or upper airway obstruction. If respiratory rate drops below 10 breaths per minute, notify prescriber, expect drug to be discontinued, and provide needed supportive care, which may include an opioid antagonist such as naloxone, as ordered.

Monitor patient for evidence of physical and psychological dependence.
WARNING Watch patient closely for evidence of serotonin syndrome, which can be life-threatening. Report mental status changes (agitation, hallucinations, coma), autonomic instability (tachycardia, labile blood pressure, hyperthermia), neuromuscular abnormalities (hyperreflexia, incoordination) or GI disturbances (nausea, vomiting or diarrhea).

Don’t stop tapentadol abruptly if used on a regular basis because withdrawal symptoms may occur.

Be aware that tapentadol shouldn’t be used during or just before labor and delivery.

PATIENT SAFTY

Instruct patient to take tapentadol exactly as prescribed and not to adjust dose or frequency without consulting prescriber.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Caution patient to avoid alcohol or other CNS depressants while taking tapentadol.

Advise patient who has been taking tapentadol regularly not to stop taking it abruptly but rather to taper drug use gradually and based on prescriber instructions to reduce the risk of withdrawal symptoms.

Category

Chemical class: Lipoglycopeptide
Therapeutic class: Antibacterial

Pregnancy category: C

Indications

To treat complicated skin and skin structure infections caused by gram-positive organisms (Staphylococcus aureus, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus anginosus group [includes S. anginosus, S. intermedius, and S. constellatus], or Enterococcus faecalis (vancomycinsusceptible isolates only)
IV:
Adults. 10 mg/kg administered over 60 min every 24 hours for 7 to 14 days
DOSAGE ADJUSTMENT For patients with creatinine clearance ot 30 to 50 ml/min/ 1.73 m2, dosage reduced to 7.5 mg/kg every 24 hours. For patient with creatinine clearance of at least 10 but less than 30 ml/min/ 1.73 m2, 10 mg/kg every 48 hours. Route Onset Peak Duration I.V. Unknown 1–2 hr 24 hr

Mechanism of Action

Inhibits cell wall synthesis and alters the permeability of bacterial membranes, causing cell wall lysis and cell death. Telavancin is a lipoglycopeptide antibacterial that’s a synthetic derivative of vancomycin.

Incompatibilities

Don’t mix telavancin with other or IV solutions containing additives. If administration must be through the same IV line, flush the line with 5% dextrose injection, 0.9% sodium chloride injection, or lactated Ringer’s injection before and after infusing telavancin.

Contraindications

Hypersensitivity to telavancin or its components

Interactions

ACE inhibitors, loop diuretics,
NSAIDs: Increased risk of nephrotoxicity known to prolong the QT interval, such as clarithromycin, disopyramide, erythromycin, quindine: Increased risk of prolonged QT interval

Side Efect

CNS: Dizziness, rigors
CV: Prolonged QT interval
EENT: Taste disturbance
GI: Abdominal pain, anorexia, diarrhea, Clostridium difficile–associated diarrhea, nausea, vomiting
GU: Elevated creatinine level, foamy urine, nephrotoxicity such as renal failure, impairment, or insufficiency
SKIN: Pruritus, rash
Other: Infusion-related reactions such as erythema or pain

Cautions

Know that telavancin isn’t recommended for patients with congenital long-QT syndrome, uncompensated heart failure, or severe left ventricular hypertrophy or who currently have a prolonged QT interval because it may prolong the QT interval, causing life-threatening complications.

Use cautiously in patients taking known to prolong the QT interval because of increased the risk of a prolonged QT interval.

Make sure woman of childbearing age has a negative pregnancy test result before starting telavancin because of risk of fetal harm.

Obtain baseline serum creatinine level before telavancin therapy starts, and monitor it throughout therapy, as ordered, because drug may cause nephrotoxicity, especially in patients with pre-existing renal disease, diabetes mellitus, congestive heart failure, or hypertension and in patients taking such nephrotoxic as NSAIDs, ACE inhibitors, and loop diuretics. If renal function declines, notify prescriber and expect to discontinue telavancin.

Dilute a 250-mg vial with 15 ml or a 750mg vial with 45 ml of a diluent such as 5% dextrose injection, sterile water for injection, or 0.9% sodium chloride injection to obtain a solution of 15 mg/ml. When ready to administer drug, further dilute doses of 150 mg to 800 mg in 100 to 250 ml of 5% dextrose injection, 0.9% sodium chloride injection, or lactated Ringer’s injection before infusion. Doses less than 150 mg or greater than 800 mg should be further diluted in a volume that yields a final concentration of 0.6 to 0.8 mg/ml.

Infuse telavancin over 60 minutes because more rapid infusion may cause a reaction like red-man syndrome, which causes flushing of upper body, urticaria, pruritus, or rash. If present, stop or slow infusion to resolve.

Use telavancin within 4 hours of the time it is reconstituted in the vial (including its transfer to an infusion bag for further dilution) if kept at room temperature and 72 hours if refrigerated. Discard if time limit exceeds these parameters.

Monitor patient for diarrhea, which may range from mild to severe and may occur up to 2 months after antibiotic is discontinued. Report diarrhea and, if C. difficile is suspected, expect telavancin to be discontinued. Provide supportive care, such as fluid and electrolyte replacement, protein supplementation, antibiotic therapy to treat C. difficile, and possibly surgical intervention, as needed.

Be aware that while telavancin doesn’t interfere with coagulation, it does interfere with certain tests used to monitor coagulation, such as PT, INR, APTT, activated clotting time, and coagualtion-based factor Xa tests. Collect blood samples for coagulation tests as close as possible to administration of next dose of telavancin to minimize interference.

PATIENT SAFTY

telavancin 985 T

Instruct women of childbearing age to use effective contraception during telavancin therapy.

Caution patient that diarrhea may occur up to 2 months after antibiotic has been discontinued and to report any persistent or severe episodes to prescriber.

Warn patient that drug may cause urine to be foamy and taste to be altered.

Advise patient to alert all prescribers that he takes telavancin because some may interact with it, causing serious adverse effects.

Category

Chemical class: Semisynthetic ketolide
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To treat mild to moderate communityacquired pneumonia caused by Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, Chlamydophila pneumoniae, or Mycoplasma pneumoniae
Adults. 800 mg daily P.O. for 7 to 10 days. Route Onset Peak Duration P.O. Unknown 1 hr Unknown

Mechanism of Action

Binds to domains II and V of the 50S ribosomal subunit in many aerobic, anaerobic, gram-positive, and gram-negative bacteria of the respiratory tract. Telithromycin may also inhibit the assembly of nascent ribosomal units. These actions inhibit RNAdependent protein synthesis in bacterial cells, causing them to die.

Contraindications

Cisapride or pimozide therapy; history of hepatitis or jaundice associated with use of telithromycin or any macrolide antibiotic; hypersensitivity to telithromycin, macrolide antibiotics, or their components; myasthenia gravis

Interactions

atorvastatin, lovastatin, midazolam, pimozide, simvastatin: Possibly increased blood levels of these cisapride, dofetilide, procainamide, quinidine: Increased risk of prolonged QT interval itraconazole,
ketoconazole: Increased blood level of telithromycin oral anticoagulants: Possibly potentiated effects of oral anticoagulants
rifampin: Decreased blood level of telithromycin sotalol: Decreased sotalol absorption
theophylline: Increased risk of adverse GI reactions

Side Efect

CNS: Dizziness, fatigue, headache, insomnia, somnolence, transient loss of consciousness, vertigo
CV: Atrial arrhythmias, prolonged QT interval, torsades de pointes
EENT: Blurred vision, difficulty focusing eyes, diplopia, dry mouth, glossitis, oral candidiasis, stomatitis
GI: Abdominal distention or pain, anorexia, constipation, diarrhea, elevated liver function test results, flatulence, fulminant hepatitis, gastroenteritis, gastritis, hepatic failure or necrosis, hepatitis, nausea, pseudomembranous colitis, taste perversion, vomiting
GU: Vaginal candidiasis, vaginitis, vaginosis (fungal)
HEME: Increased platelet count
MS: Exacerbated myasthenia gravis, muscle cramps
RESP: Acute respiratory failure
SKIN: Diaphoresis, rash
Other: Angioedema, anaphylaxis

Cautions

Be aware that telithromycin therapy shouldn’t be used in patients who have congenital prolonged QT interval or ongoing proarrhythmic conditions (such as uncorrected hypokalemia or hypomagnesemia, or serious bradycardia) or in those receiving concurrent therapy with class IA or class III antiarrhythmics because telithromycin increases the risk of QTinterval prolongation, which may lead to ventricular arrhythmias, including torsades de pointes. telithromycin 986

Before administering the first telithromycin dose, expect to obtain respiratory specimens for culture and sensitivity testing.

Monitor patient closely for diarrhea, which may indicate pseudomembranous colitis. If it occurs, notify prescriber and expect to withhold drug and give fluids, electrolytes, protein, and an antibiotic effective against Clostridium difficile.
WARNING Monitor patient’s liver studies for abnormalities, and assess patient for evidence of liver dysfunction, such as fatigue, malaise, anorexia, nausea, jaundice, acholic stools, and liver tenderness, because telithromycin may cause potentially life-threatening acute hepatic failure and severe liver damage.

PATIENT SAFTY

Stress need to take drug for prescribed duration even if patient feels better before prescription is finished.

Caution patient to avoid hazardous activities until drug’s CNS and visual effects are known. Explain that telithromycin can cause trouble focusing eyes, especially for first 30 minutes after a dose.

Instruct patient to notify prescriber if visual disturbances occur, and tell her to avoid quick changes in viewing near and distant objects.

Tell patient to alert prescriber if she faints because drug may alter heart rhythm.

Caution patient to notify prescriber immediately about fatigue, malaise, anorexia, nausea, abdominal tenderness, yellow skin, or changes in stool appearance.

Category

Chemical class: Nonpeptide angiotensin II antagonist
Therapeutic class: Antihypertensive

Pregnancy category: C

(first trimester), D (later trimesters)

Indications

To manage hypertension, alone or with other antihypertensives
Adults. Initial: 40 mg daily. Maintenance: 20 to 80 mg daily. Maximum: 80 mg daily. To reduce risk of MI, stroke, or death from cardiovascular causes in patients at high risk who are unable to take ACE inhibitors Adults age 55 and over.80 mg once daily. Route Onset Peak Duration P.O. Unknown In 4 wk Unknown

Mechanism of Action

Blocks angiotensin II from binding to receptor sites in many tissues, including vascular smooth muscle and adrenal glands. This action inhibits the vasoconstrictive and aldosterone-secreting effects of angiotensin II, which reduces blood pressure.

Contraindications

Hypersensitivity to telmisartan or its components

Interactions

digoxin: Increased peak blood digoxin level and risk of digitalis toxicity diuretics, other antihypertensives: Enhanced hypotensive effect lithium: Increased serum lithium levels and toxicity ramipril: Increased serum ramipril level; decreased telmisartan level

Side Efect

CNS: Asthenia, dizziness, fatigue, headache, syncope, weakness
CV: Atrial fibrillation, bradycardia, chest pain, congestive heart failure, hypertension, hypotension, MI, orthostatic hypotension, peripheral edema
EENT: Pharyngitis, sinusitis
GI: Abdominal pain, diarrhea, elevated liver enzyme levels, indigestion, nausea, vomiting
GU: Acute renal failure, erectile dysfunction, renal dysfunction, UTI
HEME: Anemia, eosinophilia, thrombocytopenia
MS: Back pain, leg or muscle cramps, myalgia, tendon pain, tendinitis, tenosynovitis
RESP: ACE cough, upper respiratory tract infection
SKIN: Diaphoresis, erythema, urticaria
Other: Anaphylaxis, angioedema, elevated uric acid level, flulike symptoms, hyperkalemia, hypovolemia

Cautions

Give telmisartan cautiously to patients with dehydration or hyponatremia.

Expect prescriber to add a diuretic to regimen if patient’s blood pressure isn’t well controlled by telmisartan.

Check patient’s blood pressure regularly. Be prepared to treat symptomatic hypotension by placing patient in supine position and giving normal saline solution, as ordered.

Monitor BUN and serum creatinine levels and urine output in patients with impaired renal function because they’re at increased risk for oliguria, progressive azotemia, and possibly acute renal failure.

Monitor liver function test results, as appropriate, and assess for evidence of drug toxicity in patients with severe hepatic disease because they’re at increased risk for toxicity from increased drug accumulation.

Avoid using telmisartan in pregnant women during second and third trimesters because drug can increase the risk of fetal harm.

PATIENT SAFTY

Advise patient to avoid hazardous activities until telmisartan’s CNS effects are known.

Instruct patient to change position slowly to minimize effects of orthostatic hypotension.

Urge patient to immediately notify prescriber about diarrhea, dizziness, severe nausea, or vomiting.

Instruct patient to consult prescriber before taking any new drug.

Advise patient to drink adequate amounts of fluid during hot weather and when exercising.

Advise female patients of childbearing age to notify presciber immediately about known or suspected pregnancy.

Category

Chemical class: Benzodiazepine
Therapeutic class: Sedative-hypnotic

Pregnancy category: X

Controlled substance schedule: IV

Indications

To provide short-term management of insomnia
Adults. 7.5 to 30 mg 30 min before at bedtime. Maximum: 30 mg daily.
DOSAGE ADJUSTMENT For elderly or debilitated patients, 7.5 mg 30 min before bedtime. Maximum: 15 mg daily.

Mechanism of Action

May potentiate the effects of gammaaminobutyric acid (GABA) and other inhibitory neurotransmitters by binding to specific benzodiazepine receptor sites in limbic and cortical areas of the CNS. By binding to these receptor sites, temazepam increases GABA’s inhibitory effects and blocks cortical and limbic arousal.

Contraindications

Hypersensitivity to temazepam, other benzodiazepines, or their components; pregnancy

Interactions

antihistamines (such as brompheniramine, carbinoxamine, chlorpheniramine, clemastine, cyproheptadine, diphenhydramine, trimeprazine), anxiolytics, barbiturates, general anesthetics, opioid analgesics, phenothiazines, promethazine, sedative-hypnotics, tramadol, tricyclic antidepressants: Increased sedation or respiratory depression clozapine: Risk of respiratory depression or arrest digoxin: Increased risk of elevated blood digoxin level and digitalis toxicity
flumazenil: Increased risk of withdrawal symptoms levodopa: Possibly decreased levodopa effects oral contraceptives: Decreased response to temazepam
phenytoin: Possibly phenytoin toxicity probenecid: Increased response to temazepam zidovudine: Possibly zidovudine toxicity
alcohol use: Increased CNS depression and risk of apnea smoking: Increased temazepam clearance

Side Efect

CNS: Aggressiveness, anxiety (in daytime), ataxia, complex behaviors (such as sleep driving), confusion, decreased concentration, depression, dizziness, drowsiness, euphoria, fatigue, headache, insomnia, nightmares, slurred speech, suicidal ideation, syncope, talkativeness, tremor, vertigo, wakefulness during last third of night
CV: Palpitations, tachycardia
EENT: Abnormal or blurred vision, increased salivation, throat tightness
GI: Abdominal pain, constipation, diarrhea, hepatic dysfunction, nausea, thirst, vomiting
GU: Decreased libido
HEME: Agranulocytosis, anemia, leukopenia, neutropenia, thrombocytopenia
MS: Muscle spasm or weakness
RESP: Dyspnea, increased bronchial secretions
SKIN: Diaphoresis, flushing, jaundice, pruritus, rash
Other: Anaphylaxis, angioedema, physical and psychological dependence

Cautions

Use temazepam cautiously in patients with a history of depression or suicidal thoughts.
WARNING Monitor patient closely for evidence of hypersensitivity reaction, such as dyspnea, throat tightness, nausea, vomiting, and swelling. If present, discontinue temazepam immediately, notify prescriber, and provide supportive care.

Watch patient closely for suicidal tendencies, particularly when therapy starts and dosage changes, because depression may worsen temporarily during these times and could lead to suicidal ideation.
WARNING Monitor patient for evidence of physical and psychological dependence during therapy.

Implement safety precautions, according to facility policy, especially in elderly patients, because they’re more sensitive to drug’s CNS effects.

Assess patients with respiratory depression, severe COPD, or sleep apnea for signs of ventilatory failure.

Be aware that temazepam can aggravate acute intermittent porphyria, myasthenia gravis, and severe renal impairment.

Be aware that temazepam may cause worsening psychosis or deterioration of cognition or coordination in patients with latestage Parkinson’s disease.

Be aware that drug shouldn’t be discontinued abruptly, even after only 1 to 2 weeks of therapy, because doing so may cause seizures or withdrawal symptoms, such as insomnia, irritability, and nervousness.

PATIENT SAFTY

Instruct patient to take temazepam exactly as prescribed and not to stop or change dosage without consulting prescriber.

Explain the risks associated with abrupt cessation, including abdominal cramps, acute sense of hearing, confusion, depression, nausea, numbness, perceptual disturbances, photophobia, sweating, tachycardia, tingling, trembling, and vomiting.

Advise patient to avoid consuming alcohol because it increases drug’s sedative effects and the risk of such abnormal behaviors as sleep driving.

Caution patient about possible drowsiness. Advise her to avoid potentially hazardous activities until drug’s CNS effects are known.

Urge patient to notify prescriber immediately about excessive drowsiness, nausea, and known or suspected pregnancy.

Instruct patient to stop taking temazepam and seek emergency care if she experiences difficulty breathing, throat tightness, nausea, vomiting, or abnormally swelling.

Advise patient that drug may cause abnormal behaviors during sleep, such as driving a car, eating, talking on the phone, or having sex without any recall of the event. If family notices any such behavior or patient sees evidence of such behavior upon awakening, the prescriber should be notified.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes.

Category

Chemical class: Purified glycoprotein
Therapeutic class: Thrombolytic

Pregnancy category: C

Indications

To reduce mortality associated with acute MI
I.V.INJECTION
Adults. Single bolus administered over 5 sec in individualized dosage based on patient’s weight, as follows: 30 mg (6 ml) for patients weighing less than 60 kg (132 lb); 35 mg (7 ml) for patients weighing 60 to 69 kg (132 to 152 lb); 40 mg (8 ml) for patients weighing 70 to 79 kg (154 to 174 lb); 45 mg (9 ml) for patients weighing 80 to 89 kg (176 to 196 lb); 50 mg (10 ml) for patients weighing 90 kg (198 lb) or more. Maximum: 50 mg total dose.

Mechanism of Action

Binds to fibrin and converts plasminogen to plasmin. Plasmin breaks down fibrin, fibrinogen, and other clotting factors, resulting in dissolution of a coronary artery thrombus.

Incompatibilities

Don’t administer tenecteplase through an I.V. line containing dextrose because precipitation may occur.

Contraindications

Active internal bleeding, aneurysm, arteriovenous malformation, bleeding disorders, brain tumor, history of cerebrovascular accident, hypersensitivity to tenecteplase or its components, intracranial or intraspinal surgery or trauma within past 2 months, severe uncontrolled hypertension

Interactions

abciximab, aspirin, clopidogrel, dipyridamole, heparin, oral anticoagulants, ticlopidine: Possibly increased risk of bleeding

Side Efect

CNS: Intracranial hemorrhage
EENT: Epistaxis, gingival bleeding, pharyngeal bleeding
GI: GI and retroperitoneal bleeding
GU: Genitourinary bleeding, prolonged or heavy menstrual bleeding
HEME: Hematoma
RESP: Hemoptysis
SKIN: Bleeding at puncture sites, surgical incision sites, or venous cutdown sites

Cautions

WARNING Reconstitute tenecteplase for injection immediately before use because drug contains no antibacterial preservatives. If reconstituted drug isn’t used immediately, refrigerate vial at 36° to 46° F (2° to 8° C). Discard solution if not used within 8 hours.

To reconstitute and administer drug, use supplied 10-ml syringe with dual cannula device. Withdraw 10 ml of supplied (preservative-free) sterile water for injection into syringe, and inject entire contents into vial containing tenecteplase dry powder, directing stream of diluent into powder. Gently swirl—don’t shake—vial until contents are completely dissolved. If slight foaming occurs during reconstitution, allow drug to stand undisturbed for a few minutes to allow large bubbles to dissipate. Then withdraw prescribed dose of tenecteplase from reconstituted drug in vial, using supplied syringe. Make sure that reconstituted preparation is a colorless to pale yellow transparent solution. Discard any unused solution.

Give drug as a single I.V. bolus over 5 seconds. Although supplied syringe is intended for use with needleless I.V. systems, be aware that it is also compatible with a conventional needle. Follow manufacturer’s directions for use with each system. Flush any dextrose-containing I.V. lines with saline solution before and after administering tenecteplase.
WARNING Monitor patient for evidence of GI bleeding, including bloody or black, tarry stools; bloody or coffee-ground vomitus; and severe stomach pain. Notify prescriber immediately if any of these signs or symptoms develops.

Assess tenecteplase injection site for signs and symptoms of hematoma, including deep, dark purple bruises under skin and itching, pain, redness, or swelling. Also monitor patient for superficial bleeding, delayed bleeding at puncture sites, and bleeding from surgical incisions.

Assess for signs and symptoms of intracranial bleeding (such as decreased level of consciousness), retroperitoneal bleeding (such as abdominal pain or swelling and back pain), genitourinary bleeding (such as hematuria), or respiratory tract bleeding (such as hemoptysis). Notify prescriber immediately if patient develops any of these signs or symptoms.

If serious bleeding (not controllable by local pressure) occurs, expect to discontinue concomitant heparin or oral antiplatelet therapy immediately.

If possible, avoid I.M. injections and nonessential handling of patient for first few hours after drug administration.

If arterial puncture becomes necessary during first few hours after tenecteplase administration, expect to use an upper extremity that’s accessible to manual compression. Apply pressure for at least 30 minutes after procedure, use a pressure dressing, and frequently monitor puncture site for signs of bleeding.

PATIENT SAFTY

Advise patient to immediately report any bleeding, including from nose or gums.

Instruct patient to limit physical activity during tenecteplase administration to reduce the risk of injury or bleeding.

Category

Chemical class: Quinazoline derivative
Therapeutic class: Antihypertensive, benign prostatic hyperplasia (BPH) treatment

Pregnancy category: C

Indications

To manage hypertension
Adults. Initial: 1 mg at bedtime. Maintenance: 1 to 5 mg daily as a single dose or in divided doses every 12 hr. Maximum: 20 mg daily. To treat symptomatic BPH
Adults. Initial: 1 mg at bedtime, increased in increments to 2 mg, 5 mg, and then 10 mg, as prescribed, based on symptom improvement and urine flow rate. Maintenance: 5 to 10 mg daily as a single dose or in divided doses every 12 hr. Maximum: 20 mg daily. Route Onset Peak Duration P.O. 15 min 2–3 hr 24 hr

Mechanism of Action

Blocks postsynaptic alpha1-adrenergic receptors in many tissues, including vascular smooth muscle, the bladder neck, and the prostate. This action promotes vasodilation, which reduces blood pressure and improves urine flow.

Contraindications

Hypersensitivity to terazosin, other quinazolines, or their components

Interactions

clonidine: Possibly decreased clonidine effects diuretics, other antihypertensives: Additive hypotensive effect dopamine: Risk of decreased terazosin effects and antagonized vasoconstrictive effect of dopamine (in high doses) epinephrine: Risk of decreased terazosin effects, possibly severe hypotension and tachycardia indomethacin, other
NSAIDs: Altered terazosin effects related to sodium and fluid retention methoxamine, phenylephrine: Decreased vasopressor effects, and shortened duration of action of these phosphodiesterase-5 inhibitors, verapamil: Additive blood pressure–lowering effects and symptomatic hypotension sympathomimetics: Decreased terazosin effects

Side Efect

CNS: Asthenia, dizziness, headache, lethargy, nervousness, paresthesia, somnolence, syncope, vertigo
CV: Chest pain, hypotension, orthostatic hypotension, palpitations, peripheral edema, sinus tachycardia
EENT: Blurred vision, dry mouth, intraoperative floppy iris syndrome, nasal congestion, sinusitis
GI: Constipation, diarrhea, nausea, vomiting
MS: Arthralgia, back pain terazosin hydrochloride 991 T
Other: Flulike symptoms, weight gain

Cautions

Be aware that prostate cancer should be ruled out before giving terazosin for BPH.

Expect prescriber to reduce terazosin dosage if a diuretic or another antihypertensive is added to patient’s regimen.

Monitor blood pressure 2 to 3 hours after initial dose because of possible first-dose hypotension and again after 24 hours to evaluate patient’s response.

If patient requires administration by feeding tube, place capsule in 60 ml of warm tap water. Stir until capsule shell dissolves and liquid contents are released into water (5 to 10 minutes).

Be aware that elderly patients may have exaggerated hypotension and other

Side Efect

.

PATIENT SAFTY

Instruct patient to take terazosin at the same time each night.

Explain possible first-dose hypotension. Advise patient to change position and rise slowly to prevent syncope early in therapy. Suggest sitting or lying down if dizziness or light-headedness occurs.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Instruct patient to notify prescriber if she misses several doses in a row; caution her against resuming therapy at previous dose.

Inform patient that drug may take 2 to 6 weeks to improve urinary hesitancy.

Advise patient to avoid alcohol use, prolonged standing, and excessive exercise or exposure to hot weather because these activities can worsen orthostatic hypotension.

Stress the importance of regular follow-up visits with prescriber to evaluate patient’s response to drug.

Category

Chemical class: Allylamine derivative
Therapeutic class: Antifungal

Pregnancy category: B

Indications

To treat onychomycosis of fingernails and toenails Adults and adolescents. 125 mg b.i.d. or 250 mg daily for 6 to 12 wk.
DOSAGE ADJUSTMENT For patients with stable chronic hepatic dysfunction or renal dysfunction (creatinine clearance less than 50 ml/min/1.73 m2or serum creatinine greater than 3.4 mg/dl), dosage reduced by 50%.

Mechanism of Action

Inhibits the conversion of squalene monooxygenase to squalene epoxidase, a key enzyme in fungal biosynthesis. The resulting squalene accumulation weakens cell membranes and creates a deficiency of ergosterol, the fungal membrane component necessary for normal fungal growth.

Contraindications

Hypersensitivity to terbinafine or its components

Interactions

beta blockers, MAO inhibitors (type B), selective serotonin reuptake inhibitors, tricyclic antidepressants: Possibly increased blood levels of these cimetidine, other hepatic enzyme inhibitors: Significantly decreased terbinafine clearance, possibly increased

Side Efect

hepatotoxic : Increased risk of hepatotoxicity
rifampin: Increased clearance and decreased effectiveness of terbinafine caffeine: Decreased caffeine clearance
alcohol use: Increased risk of severe hepatitis

Side Efect

CNS: Headache
EENT: Taste perversion
GI: Abdominal pain, anorexia, diarrhea, elevated liver function test results, flatulence, hepatic failure, indigestion, nausea, vomiting
SKIN: Cutaneous lupus erythematosus, terbinafine hydrochloride 992 pruritus, rash, urticaria
Other: Angioedema, systemic lupus erythematosus

Cautions

Because terbinafine has been linked to serious adverse hepatic effects, expect to send nail specimens for laboratory testing to confirm onychomycosis before starting therapy.

Be aware that drug shouldn’t be given to patients with chronic or active hepatic disease or renal impairment.

Monitor patient for hepatic failure (anorexia, dark urine, fatigue, jaundice, nausea, pale stools, right upper abdominal pain, and vomiting). Expect to stop drug and obtain liver function tests if these problems develop.

PATIENT SAFTY

Instruct patient to space terbinafine doses evenly if taking drug more than once a day.

Stress the need to complete the full course of terbinafine therapy to prevent relapse of infection.

Discourage consumption of alcohol during therapy.

Tell patient to contact prescriber if onychomycosis doesn’t improve in a few weeks.

Category

Chemical class: Sympathomimetic amine
Therapeutic class: Bronchodilator

Pregnancy category: B

Indications

To prevent or reverse bronchospasm from asthma, bronchitis, or emphysema (BRETHINE, BRICANYL) Adults and adolescents age 15 and over. 2.5 to 5 mg t.i.d. at 6-hr intervals while awake. Maximum: 15 mg daily. Children ages 12 to 15. 2.5 mg t.i.d. at 6-hr intervals while awake. Maximum: 7.5 mg daily. Children ages 6 to 11. 50 to 75 mcg/kg t.i.d. at 6-hr intervals while awake. Maximum: 150 mcg/kg/dose or 5 mg daily. SUBCUTANEOUS INJECTION(BRICANYL) Adults and children age 12 and over. Initial: 0.25 mg, repeated in 15 to 30 min as prescribed. Maximum: 0.5 mg/4-hr period. Children ages 6 to 12. 5 to 10 mcg (0.005 to 0.01 mg)/kg every 15 to 20 min, up to 3 doses. Maximum: 400 mcg (0.4 mg)/dose. INHALATION AEROSOL(BRETHAIRE) Adults and children. 2 inhalations (400 mcg) every 4 to 6 hr, as needed and as prescribed. INHALATION AEROSOL(BRICANYL TURBUHALER) Adults and children. 1 inhalation (500 mcg), repeated after 5 min, as needed and as prescribed. Maximum: 6 inhalations daily. Route Onset Peak Duration P.O. 30–90 2–3 hr 4–8 hr min SubQ 15–30 30–60 min 1.5–4 hr min Inhalation In 5 min 30–90 min 3–6 hr

Mechanism of Action

Stimulates beta2-adrenergic receptors in the lungs, which is believed to increase production of cAMP. The increased cAMP level relaxes bronchial smooth muscles, thereby increasing bronchial airflow and relieving bronchospasm.

Contraindications

Hypersensitivity to terbutaline, other sympathomimetic amines, or their components

Interactions

antihypertensives, diuretics: Decreased antihypertensive effect
beta blockers: Mutual inhibition of therapeutic effects, increased risk of bronchospasm CNS stimulants: Additive CNS stimulation, possibly resulting in adverse effects digoxin: Increased risk of arrhythmias, possibly digitalis toxicity halogenated anesthetics: Possibly ventricular arrhythmias
MAO inhibitors: Possibly potentiated action of terbutaline; headache, hyperpyrexia, hypertension, possible hypertensive crisis maprotiline, tricyclic antidepressants: terbutaline sulfate 993 T Possibly potentiated action of terbutaline nitrates: Decreased effectiveness of nitrates ritodrine: Increased effects of either drug and potential for adverse effects sympathomimetics: Increased CNS stimulation and risk of adverse cardiovascular effects, including prolonged QT interval thyroid hormones: Increased effects of either drug, risk of coronary insufficiency in patients with coronary artery disease xanthines (theophylline): Increased CNS stimulation and other additive toxic effects caffeine: Increased CNS stimulation and other additive toxic effects

Side Efect

CNS: Anxiety, dizziness, drowsiness, headache, insomnia, light-headedness, nervousness, restlessness, tremor, weakness
CV: Chest pain, irregular heartbeat, palpitations, tachycardia
EENT: Dry mouth, taste perversion
ENDO: Hyperglycemia
GI: Heartburn, nausea, vomiting
MS: Muscle spasms
RESP: Dyspnea
SKIN: Diaphoresis, flushing, rash

Cautions

Use terbutaline cautiously in patients with cardiovascular disease because drug can adversely affect cardiovascular function. Monitor patient’s heart rate and rhythm and blood pressure, and assess for chest pain.

For subcutaneous use, inject into lateral deltoid area.

Assess patient’s respiratory rate, depth, and quality; oxygen saturation; and activity tolerance at regular intervals because continuous use of beta2-agonists for 12 months or longer accelerates the decline in pulmonary function.

PATIENT SAFTY

Teach patient how to use terbutaline aerosol inhaler or give subcutaneous injection, as needed.

Instruct patient not to increase dose or frequency without consulting prescriber.

Urge patient to seek immediate medical attention if symptoms worsen.

Inform patient that she may experience transient nervousness or tremors during terbutaline therapy.

Category

Chemical class: Recombinant human parathyroid hormone (PTH)
Therapeutic class: Bone growth and density regulator

Pregnancy category: C

Indications

To treat osteoporosis in postmenopausal women and primary or hypogonadal osteoporosis in men at high risk for fracture; to treat men and women with glucocorticoid-induced osteoporosis at high risk for fracture SUBCUTANEOUS INJECTION
Adults. 20 mcg daily for up to 2 yr. Route Onset Peak Duration SubQ 2 hr 4–6 hr 16–24 hr

Contraindications

Hypersensitivity to teriparatide or its components

Interactions

digitalis glycosides: Possibly increased risk of digitalis toxicity

Side Efect

CNS: Asthenia, depression, dizziness, headache, insomnia, paresthesia, syncope, vertigo
CV: Angina pectoris, chest pain, hypertension, transient orthostatic hypotension
EENT: Pharyngitis, rhinitis, taste perversion, tooth disorder
ENDO: Transient hypoparathyroidism
GI: Constipation, diarrhea, indigestion, vomiting
MS: Arthralgia, muscle cramps or spasms in back or leg, neck pain
RESP: Cough, dyspnea, pneumonia
SKIN: Diaphoresis, pruritus, rash, urticaria
Other: Angioedema, generalized pain, injection site reactions (erythema, localized bruising, minor bleeding, pain, pruritus, swelling), transient hypercalcemia or hypocalcemia

Cautions

WARNING Be aware that teriparatide shouldn’t be used to treat patients at risk for osteosarcoma (such as those with Paget’s disease or a metabolic bone disease other than osteoporosis), unexplained elevations of alkaline phosphatase, open epiphyses, or prior skeletal radiation or malignancy.
WARNING Be aware that patients with hypercalcemia shouldn’t receive teriparatide because drug may worsen hypercalcemia.

Use drug cautiously in patients with active or recent urolithiasis because drug could worsen this condition.

Monitor patient closely for allergic reactions because teriparatide is a peptide agent.

Monitor patient’s blood calcium level, and notify prescriber of any elevation; in persistent hypercalcemia, the drug may need to be stopped.

Monitor patient’s blood pressure during the first several doses of drug therapy because of a risk of transient orthostatic hypotension. If this occurs, place patient in a reclining position and alert prescriber.

PATIENT SAFTY

Teach patient how to administer teriparatide by subcutaneous injection and how to properly use the delivery pen device and dispose of needles. Advise her not to share pen device with others.

Inform patient that each delivery pen can be used for up to 28 days after the first injection but then should be discarded even if it still contains solution.

Instruct patient to store the delivery pen in the refrigerator and to recap it when not in use to protect it from damage and light.

Tell patient that delivery pen may be used immediately after removal from refrigerateriparatide 995 T

Mechanism of Action

Teriparatide, which contains recombinant PTH, stimulates new bone growth and increases bone density. In a patient with osteoporosis, bone density and mass are diminished by an imbalance between bone destruction and formation. Normally, osteoclasts break down and resorb bone, leaving behind a cavity in a section of bone. Then bone-building cells, called osteoblasts, line the walls of the cavity and stimulate new bone formation. PTH stimulates these actions by attaching to receptors on osteoclasts and osteoblasts, as shown below. Teriparatide binds to cell-surface receptors on osteoblasts and preferentially stimulates osteoblastic over osteoclastic activity. Also, the drug increases the amount of circulating calcium available for bone formation by increasing the intestinal absorption of calcium and phosphate, thus enhancing the rate of calcium resorption from bone, increasing the reabsorption of calcium, and inhibiting the reabsorption of phosphate in the kidneys. These actions stimulate new bone formation and increase bone density to reduce osteoporotic bone changes. tor and should be put back in refrigerator as soon as the injection is given.

Instruct patient to inject drug into thigh or abdominal wall and to rotate injection sites.

Caution patient to administer drug in a room where she can immediately sit or lie down if light-headedness or palpitations occur. Advise her to notify prescriber if these symptoms persist or worsen.

Instruct patient to notify prescriber of persistent symptoms of hypercalcemia, such as nausea, vomiting, constipation, lethargy, and muscle weakness.

Caution patient about potential developing osteosarcoma.

Category

Chemical class: Chlortetracycline derivative
Therapeutic class: Antibiotic

Pregnancy category: D

Indications

To treat actinomycosis caused by susceptible organisms , ORAL SUSPENSION, Adults and adolescents. 250 to 500 mg every 6 hr or 500 to 1,000 mg every 12 hr. Maximum: 4 g daily. Children age 8 and over.6.25 to 12.5 mg/kg every 6 hr or 12.5 to 25 mg/kg every 12 hr. To treat acne vulgaris , ORAL SUSPENSION, Adults and adolescents. Initial: 500 to 2,000 mg daily in divided doses until improvement occurs (usually in 3 wk); then dosage reduced gradually. Maintenance: 125 to 1,000 mg daily. Maximum: 4 g daily. To treat brucellosis caused by susceptible organisms , ORAL SUSPENSION, Adults and adolescents. 500 mg every 6 hr for 3 wk, given with 1 g of streptomycin I.M. every 12 hr in week 1 and daily in week 2. Maximum: 4 g daily. Children ages 8 to 12. 6.25 to 12.5 mg/kg every 6 hr, or 12.5 to 25 mg/kg every 12 hr. To treat gonorrhea caused by Neisseria gonorrhoeae , ORAL SUSPENSION, Adults and adolescents. 1,500 mg, then 500 mg every 6 hr for 5 days. Maximum: 4 g daily. To treat syphilis caused by Treponema pallidum , ORAL SUSPENSION, Adults and adolescents. 500 mg every 6 hr for 15 days (for early syphilis) or 30 days (for late syphilis). Maximum: 4 g daily. Children ages 9 to 12. 6.25 to 12.5 mg/kg every 6 hr, or 12.5 to 25 mg/kg every 12 hr. To treat uncomplicated endocervical, rectal, or urethral infections caused by Chlamydia trachomatis , ORAL SUSPENSION, Adults and adolescents. 500 mg q.i.d. for at least 7 days. Maximum: 4 g daily.
DOSAGE ADJUSTMENT For patients with renal impairment, dosage possibly reduced because of extended half-life.

Mechanism of Action

Exerts a bacteriostatic effect against a wide variety of gram-positive and gram-negative organisms by passing through the bacterial lipid bilayer, where it binds reversibly to 30S ribosomal subunits. Bound tetracycline blocks the binding of aminoacyl transfer RNA to messenger RNA, thus inhibiting bacterial protein synthesis.

Contraindications

Hypersensitivity to tetracycline or its components

Interactions

aluminum-, calcium-, or magnesium-containing antacids; iron supplements (oral); magnesium-containing laxatives; magnesium salicylate; multivitamins (containing manganese or zinc salts); sodium bicarbonate: Possibly impaired absorption of oral tetracycline and formation of nonabsorbable complexes cholestyramine, colestipol: Possibly impaired absorption of oral tetracycline digoxin: Possibly increased digoxin level
methoxyflurane: Possibly nephrotoxicity oral contraceptives (containing estrogen): tetracycline hydrochloride 996 Possibly reduced contraceptive reliability and increased risk of breakthrough bleeding (with long-term tetracycline use) penicillins: Possibly decreased bactericidal effect of penicillins vitamin A: Possibly benign intracranial hypertension dairy products and other : Possibly impaired absorption of oral tetracycline

Side Efect

CNS: Dizziness, light-headedness, unsteadiness
EENT: Darkened or discolored tongue, enamel hypoplasia, oral candidiasis, tooth discoloration (in children)
GI: Abdominal pain, diarrhea, hepatotoxicity, nausea, rectal candidiasis, vomiting
GU: Vaginal candidiasis
SKIN: Photosensitivity

Cautions

Avoid giving tetracycline to children under age 8 because drug may cause permanent brown or yellow tooth discoloration and enamel hypoplasia.

Be aware that tooth discoloration and enamel hypoplasia may occur in breastfeeding infants, along with inhibition of linear skeletal growth, oral and vaginal candidiasis, and photosensitivity.

To reduce the risk of esophageal irritation or ulceration, avoid bedtime dosing of tetracycline for patient with esophageal obstruction or compression.

Assess for photosensitivity, which can develop within a few minutes or up to several hours after exposure to sunlight or other ultraviolet (UV) light. Effects may last for 1 to 2 days after discontinuation of drug.

Be aware that citric acid in tetracycline preparations may accelerate drug deterioration and that using outdated drug may cause Fanconi’s syndrome, characterized by multiple defects in renal tubular function. Symptoms include acidosis, bicarbonate wasting, glycosuria, hypokalemia, osteomalacia, and phosphaturia.

PATIENT SAFTY

Instruct patient to take oral tetracycline at least 1 hour before meals or 2 hours after meals because dairy products and some may interfere with absorption.

Advise patient to take each dose with a full glass of water while in an upright position to avoid esophageal or GI irritation.

Instruct patient taking oral suspension to shake container well before measuring dose and to use a calibrated measuring device.

Advise patient to avoid taking other , including OTC antacids and other preparations, within 3 hours of oral tetracycline.

Urge patient to complete entire course of tetracycline therapy even if she feels better.

Caution her to avoid direct sunlight or UV light and to wear sunscreen when outdoors.

Advise women who use oral contraceptives containing estrogen to use another method of contraception while taking tetracycline because contraceptives may be less effective.

Stress the need to discard outdated tetracycline because of the risk of toxic effects.

Encourage patient to take safety precautions if she experiences dizziness or other adverse CNS reactions.

Category

Chemical class: Glutamic-acid derivative
Therapeutic class: Anti-inflammatory, immuno-modulator

Pregnancy category: X

Indications

To treat acute cutaneous erythema nodosum leprosum Adults and adolescents. 100 to 400 mg daily at bedtime or at least 1 hr after the evening meal. Usual: 200 mg.
DOSAGE ADJUSTMENT For patients weighing less than 50 kg (110 lb), dosage started at 100 mg. To prevent or suppress recurrence of cutaneous erythema nodosum leprosum Adults and adolescents. Minimum dosage necessary to control reaction; dosage tapered every 3 to 6 mo in increments of 50 mg every 2 to 4 wk, as prescribed. thalidomide 997 T

Mechanism of Action

Suppresses the production of tumor necrosis factor-alpha, which reduces neutrophils and CD4 T cells in erythema nodosum leprosum lesions, thus preventing or controlling symptoms.

Contraindications

Hypersensitivity to thalidomide or its components; men, regardless of history of vasectomy, who refuse to wear latex condom during intercourse with women of childbearing age; pregnancy; women of childbearing age who aren’t using two reliable contraceptive methods or aren’t abstaining from heterosexual intercourse

Interactions

antihistamines, anxiolytics, barbiturates, chlorpromazine, CNS depressants, hypnotics, opioid analgesics, reserpine, sedatives: Increased CNS depression chloramphenicol, cisplatin, dapsone, didanosine, ethambutol, ethionamide, hydralazine, isoniazid, lithium, metronidazole, nitrofurantoin, nitrous oxide, other associated with peripheral neuropathy, phenytoin, stavudine, vincristine, zalcitabine: Increased risk of peripheral neuropathy
alcohol use: Increased CNS depression

Side Efect

CNS: Agitation, anxiety, asthenia, chills, confusion, depression, dizziness, drowsiness, fatigue, fever, headache, insomnia, lethargy, loss of consciousness, malaise, mood changes, nervousness, paresthesia, peripheral neuropathy, seizures, somnolence, status epilepticus, stupor, syncope, tremor, vertigo
CV: Arrhythmias, bradycardia, embolism, hyperlipidemia, hypertension, orthostatic hypotension, peripheral edema, tachycardia, thrombosis
EENT: Dry mouth, oral candidiasis, pharyngitis, rhinitis, sinusitis, tooth pain
ENDO: Hypothyroidism
GI: Abdominal pain, anorexia, constipation, diarrhea, elevated liver function test results, flatulence, hepatic dysfunction, increased appetite, intestinal perforation, nausea, vomiting
GU: Albuminuria, elevated creatinine level, hematuria, impotence
HEME: Anemia, decreased platelets count, leukopenia, neutropenia, prolonged PT
MS: Arthralgia, back or bone pain, muscle weakness, myalgia, neck pain or rigidity
RESP: Cough, dyspnea, pleural effusion, pulmonary embolism
SKIN: Acne, dermatitis, diaphoresis, dryness, erythema multiforme, photosensitivity, pruritus, rash
Other: Facial edema, hypercalcemia, hyperkalemia, hypocalcemia, hypokalemia, hyponatremia, increased alkaline phosphatase level, lymphadenopathy, pain (generalized), tumor lysis syndrome, weight loss or gain

Cautions

Be aware that all patients receiving thalidomide must complete an informed consent form and participate in a confidential monitoring registry. Thalidomide may be obtained only through physicians and pharmacies registered in the System for Thalidomide Education and Prescribing Safety (STEPS) Program, a comprehensive safety program designed to prevent fetal exposure to thalidomide. Thalidomide may be dispensed only in original packaging and in no more than a 28-day supply. Prescriptions older than 7 days may not be filled.

Be aware that female patients of childbearing age must use two contraceptive methods during therapy. Pregnancy testing must be performed 24 hours before starting thalidomide, weekly during first month of therapy, then monthly thereafter in women with regular menstrual cycles or every 2 weeks in women with irregular menstrual cycles.
WARNING Be aware that thalidomide shouldn’t be given to pregnant patient. A single dose may cause severe birth defects or fetal death.

Assess patient’s medication history for use of carbamazepine, griseofulvin, HIV-protease inhibitors, modafinil, penicillins, phenytoin, rifabutin, rifampin, and the herbal remedy St. John’s wort. These products can decrease the effectiveness of hormonal contraceptives during thalidomide therapy.
WARNING Monitor patient closely for evithalidomide 998 dence of a venous thromboembolic event (shortness of breath, chest pain, or arm or leg swelling). Notify prescriber immediately and expect to assist with diagnostic studies to confirm suspicions and provide treatment, as ordered.

To minimize sedative effect, give thalidomide in divided doses t.i.d. or q.i.d., as prescribed, with larger dose in the evening.

Assess for early signs of peripheral neuropathy (muscle cramps, numbness and tingling in toes and fingers, pain or superficial sensory loss in feet or hands) in patients receiving long-term thalidomide therapy. Early detection and drug discontinuation, as pre-scribed, prevents further damage and increases the chance for reversal.

Expect to stop thalidomide if absolute neutrophil count is less than 750/mm3. Routine monitoring of WBC count is recommended every other week for first 3 months of treatment in HIV-positive and other immunosuppressed patients and monthly in immunocompetent patients.

PATIENT SAFTY

Instruct patient to have thalidomide prescription filled promptly because prescriptions more than 7 days old may not be filled.

Urge patient to take drug exactly as prescribed.

Inform female patient that drug will harm a fetus, and stress the need to avoid pregnancy. Tell her that pregnancy tests will be done before and frequently during therapy.

Instruct female patient to abstain from sexual intercourse or to use two reliable methods of birth control simultaneously, starting 4 weeks before drug therapy and continuing for up to 4 weeks after therapy has been completed. One contraceptive method must be highly effective, such as an intrauterine device, oral contraceptive, or tubal ligation; the other may be a cervical cap, diaphragm, or latex condom.
WARNING Inform male patient, even one who has had a vasectomy, that he must use barrier contraception (latex condom) when having sexual intercourse with a woman of childbearing age.

Caution patient to avoid hazardous activities until drug’s CNS effects are known.

Suggest changing positions slowly to minimize effects of orthostatic hypotension.

Instruct patient to immediately report signs of peripheral neuropathy, including numbness, pain, or tingling in feet and hands.

Inform HIV-positive patient of the need for viral-load testing after first and third months of therapy and then every 3 months.

Urge patient to avoid using alcohol and donating blood or sperm during therapy.

Category

Chemical class: Xanthine derivative
Therapeutic class: Bronchodilator

Pregnancy category: C

Indications

As loading dose to treat reversible airway obstruction in patients not currently receiving theophylline , ELIXIR,, SYRUP, Adults and children. 5 mg/kg as a single dose.
IV: Adults and children. 5 mg/kg infused over 20 to 30 min. As partial loading dose to treat reversible airway obstruction in patients currently receiving theophylline , ELIXIR,, SYRUP, ,
IV: Adults and children. Individualized dosage based on blood theophylline level, as pretheophylline 999 T scribed. Loading dose based on principle that 0.5 mg/kg of theophylline will produce a 1-mcg/ml increase in blood theophylline level. To provide maintenance treatment of reversible airway obstruction associated with asthma or COPD , Adults and children weighing more than 45 kg (99 lb). Initial: 300 mg daily in equally divided doses every 6 to 8 hr; after 3 days, if tolerated, increased to 400 mg daily in divided doses every 6 to 8 hr; after 3 more days, if tolerated, increased to 600 mg daily in divided doses every 6 to 8 hr. Dosages above 600 mg daily are based on blood theophylline level and clinical response. Children age 1 and over weighing 45 kg or less.Initial: 12 to 14 mg/kg daily up to maximum of 300 mg daily in equally divided doses every 4 to 6 hr; after 3 days, if tolerated, increased to 16 mg/kg up to maximum of 400 mg daily in equally divided doses every 4 to 6 hr; after 3 more days, if tolerated, 20 mg/kg daily up to maximum of 600 mg daily in equally divided doses every 4 to 6 hr. Dosages above 600 mg daily are based on blood theophylline level and clinical response. ELIXIR
Adults. Initial: 300 mg daily in equally divided doses every 6 to 8 hr; after 3 days, if tolerated, increased to 400 mg daily in divided doses every 6 to 8 hr; after 3 more days, if tolerated, increased to 600 mg daily in divided doses every 6 to 8 hr. Dosages above 600 mg daily are based on blood theophylline level and clinical response. OR Adults and children weighing 45 kg or more. Initial: 300 mg daily in equally divided doses every 8 to 12 hr; after 3 days, if tolerated, increased to 400 mg daily in divided doses every 8 to 12 hr; after 3 more days, if tolerated, increased to 600 mg daily in divided doses every 8 to 12 hr. Dosages above 600 mg daily are based on blood theophylline level and clinical response. Children age 1 and over weighing less than 45 kg. Initial: 12 to 14 mg/kg daily up to maximum of 300 mg daily in equally divided doses every 8 to 12 hr; after 3 days, if tolerated, increased to 16 mg/kg up to maximum of 400 mg daily in equally divided doses every 8 to 12 hr; after 3 more days, if tolerated, dosage increased to 20 mg/kg daily up to maximum of 600 mg daily in equally divided doses every 8 to 12 hr. Dosages above 600 mg daily are based on blood theophylline level and clinical response.

ORALL

, SYRUP Adults and children weighing more than 45 kg. Initial: 300 mg daily in equally divided doses every 6 to 8 hr; after 3 days, if tolerated, increased to 400 mg daily in divided doses every 6 to 8 hr; after 3 more days, if tolerated, increased to 600 mg daily in divided doses every 6 to 8 hr. Dosages above 600 mg daily are based on blood theophylline level and clinical response. Children age 1 and over weighing 45 kg or less. Initial: 12 to 14 mg/kg daily up to maximum of 300 mg daily in equally divided doses every 4 to 6 hr; after 3 days, if tolerated, increased to 16 mg/kg up to a maximum of 400 mg daily in equally divided doses every 4 to 6 hr; after 3 more days, if tolerated, dosage increased to 20 mg/kg daily up to maximum of 600 mg daily in equally divided doses every 4 to 6 hr. Dosages above 600 mg daily are based on blood theophylline level and clinical response. Full-term infants ages 26 to 52 weeks. Dosage individualized in mg/kg daily, as prescribed, and administered in equally divided doses every 6 hr. Full-term infants up to age 26 weeks. Dosage individualized in mg/kg daily, as prescribed, and administered in equally divided doses every 8 hr. Premature infants age 24 days and over. 1.5 mg/kg every 12 hr. Premature infants under age 24 days. 1 mg/kg every 12 hr.
IV: Adults and adolescents age 16 and over. 0.4 mg/kg/hr for nonsmokers, 0.7 mg/kg/hr for smokers.
DOSAGE ADJUSTMENT For elderly patients and adults with cardiac decompensation, cor pulmonale, or hepatic impairment, I.V. dosage reduced to 0.2 mg/kg/hr. Children ages 9 to 16. 0.7 mg/kg/hr. Children ages 1 to 9. 0.8 mg/kg/hr. Full-term infants up to age 1. Dosage inditheophylline 1000 vidualized in mg/kg daily as prescribed.

Mechanism of Action

Inhibits phosphodiesterase enzymes, causing bronchodilation. Normally, these enzymes inactivate cAMP and cGMP, which are responsible for bronchial smoothmuscle relaxation. Theophylline also may cause calcium translocation, antagonize prostaglandins and adenosine receptors, stimulate catecholamines, and inhibit cGMP metabolism.

Incompatibilities

Don’t mix parenteral theophylline solution with any additives. Don’t infuse theophylline through same I.V. line as Hetastarch (Hespan), a colloidal plasma volume expander, which is incompatible with theophylline.

Contraindications

Hypersensitivity to theophylline or its components, peptic ulcer disease, uncontrolled seizure disorder

Interactions

adenosine: Decreased adenosine effectiveness allopurinol, cimetidine, ciprofloxacin, clarithromycin, disulfiram, enoxacin, erythromycin, fluvoxamine, interferon alpha (human recombinant), methotrexate, mexiletine, pentoxifylline, propafenone, propranolol, tacrine, thiabendazole, ticlopidine, troleandomycin, verapamil: Increased blood theophylline level and risk of toxicity aminoglutethimide, carbamazepine, isoproterenol (I.V.), moricizine, oral contraceptives (containing estrogen), phenobarbital, phenytoin,
rifampin: Decreased blood theophylline level and possibly drug effectiveness benzodiazepines: Possibly reversal of benzodiazepine sedation
beta blockers: Possibly decreased bronchodilator effect of theophylline ephedrine: Increased adverse effects, including insomnia, nausea, and nervousness halothane anesthetics: Increased risk of ventricular arrhythmias ketamine: Lowered seizure threshold lithium: Decreased lithium effectiveness neuromuscular blockers: Possibly antagonized neuromuscular blockade sucralfate: Decreased absorption of oral theophylline high-carbohydrate, low-protein diet: Possibly decreased theophylline elimination low-carbohydrate, high-protein diet; daily intake of charbroiled beef: Possibly increased theophylline elimination
alcohol use: Increased blood theophylline level and risk of toxicity smoking: Increased drug clearance, decreased drug effectiveness

Side Efect

CNS: Agitation, anxiety (I.V. form), behavioral changes, confusion, disorientation, headache, insomnia, nervousness, seizures, tremor
CV: Hypotension, tachycardia, ventricular arrhythmias
ENDO: Hyperglycemia
GI: Abdominal pain, diarrhea, heartburn, nausea, vomiting
GU: Increased urine output
Other: Hypercalcemia

Cautions

Be aware that ideal body weight is used to calculate theophylline dosages because drug doesn’t bind well in body fat.

Be aware that capsules and tablets shouldn’t be used for oral loading doses.

Infuse theophylline loading dose, bolus, or intermittent infusion at a rate that doesn’t exceed 25 mg/min.

Administer continuous theophylline infusion with rate-controlled infusion device.

Monitor blood theophylline level, as ordered, to gauge therapeutic level and detect toxicity.

Frequently assess heart rate and rhythm because theophylline can exacerbate existing arrhythmias.

Be especially alert for signs of toxicity in patient with acute pulmonary edema, hypothyroidism, influenza vaccination, prolonged fever, sepsis with multiple organ failure, shock, or viral pulmonary infection because of decreased drug clearance.

Monitor blood theophylline level in patients with uncorrected acidemia because they have an increased risk of toxicity. theophylline 1001 T

Expect patient with cystic fibrosis or hyperthyroidism to have increased theophylline clearance and decreased drug effectiveness. Monitor blood theophylline level, as ordered.

Suspect toxicity if patient experiences vomiting, and be prepared to obtain blood theophylline level.

PATIENT SAFTY

Instruct patient to swallow theophylline tablets whole and not to chew or crush them, unless scored for breaking.

Explain that patient may open capsules and mix contents with soft food but that she shouldn’t chew or crush granules.

Instruct patient to take drug with a full glass of water on an empty stomach (30 to 60 minutes before meals or 2 hours after meals). However, suggest that she take drug with food or antacids if GI distress occurs.

Encourage patient to take drug at the same times every day.

Advise patient to notify prescriber if she develops a fever, makes a significant dietary change, or starts or stops smoking or taking other because these factors may alter blood theophylline level.

Tell female patient to notify prescriber if she is or cold be pregnant.

Category

Chemical class: Piperazine phenothiazine
Therapeutic class: Antiemetic

Pregnancy category: Not rated

Indications

To treat nausea and vomiting ,
I.M.INJECTION, SUPPOSITORIES Adults and adolescents. 10 mg once daily to t.i.d. Maximum: 30 mg daily.

Mechanism of Action

Relieves nausea and vomiting by centrally blocking dopamine receptors in the medullary chemoreceptor trigger zone.

Contraindications

Breast-feeding; coma; hypersensitivity to thiethylperazine, sulfites, tartrazine dye, or their components; jaundice; severe CNS depression

Interactions

aluminumor magnesium-containing antacids, antidiarrheals (adsorbent): Decreased absorption of thiethylperazine anticonvulsants (including barbiturates): Lowered seizure threshold antihistamines, tricyclic antidepressants: Additive CNS and GI effects, including ileus and severe constipation antihypertensives: Enhanced hypotensive effect of both antimuscarinics (including antiparkinsonian , MAO inhibitors, meperidine, and phenothiazines): Additive GI effects, including ileus and severe constipation appetite suppressants: Decreased anorectic effect barbiturates, benzodiazepines, CNS depressants, general anesthetics, opioid analgesics: Additive CNS effects
beta blockers: Increased blood levels of both ; additive hypotensive effects; possibly arrhythmias, irreversible retinopathy, and tardive dyskinesia bromocriptine: Possibly decreased effectiveness of bromocriptine hepatotoxic : Increased risk of hepatotoxicity levodopa: Decreased effectiveness of levodopa lithium: Possibly acute encephalopathy methoxsalen, porfimer: Possibly increased photosensitivity metrizamide: Increased risk of seizures ototoxic : Possibly masked symptoms of ototoxicity (dizziness, tinnitus, and vertigo)
phenytoin: Increased risk of phenytoin toxicity
quinidine: Possibly adverse cardiac effects
riboflavin: Increased requirements for riboflavin sympathomimetics: Reduced vasopressor response and duration of action of sympathomimetics
tramadol: Additive CNS effects, increased risk of seizures
alcohol use: Additive CNS effects

Side Efect

CNS: Confusion, dizziness, EEG abnormalities, extrapyramidal reactions (dystonia, pseudoparkinsonism), sedation
CV: ECG changes, hypotension, orthostatic hypotension, tachycardia
EENT: Blurred vision, dry mouth
ENDO: Gynecomastia
GI: Constipation, increased appetite
GU: Darkened urine, ejaculation disorders, menstrual irregularities, urine retention
HEME: Agranulocytosis, leukopenia (transient)
SKIN: Contact dermatitis, photosensitivity
Other: Weight gain

Cautions

Avoid using thiethylperazine in patients with neurologic impairment because drug can disrupt central temperature regulation.

Avoid inadvertent I.V. administration of thiethylperazine; injection is for I.M. administration only.

Keep patient in recumbent position for 30 to 60 minutes after I.M. injection to minimize the risk of hypotension.

Be aware that parenteral preparations contain sulfites and that tablets contain tartrazine dye.

Moisten suppository with water or watersoluble lubricant before insertion. If suppository has softened excessively, chill for 30 minutes or run under cold water before removing wrapper.

Avoid skin contact with drug to prevent contact dermatitis.

Because thiethylperazine may cause reactions from anticholinergic effects and adrenergic blockade, assess for blurred vision, constipation, dry mouth, impotence, urine retention (from cholinergic activity) and priapism (from alphaadrenergic blockade).

During prolonged therapy, assess for visual disturbances because drug may cause corneal keratopathy and retinal discoloration (pigmentary retinopathy).
WARNING Be aware that thiethylperazine may cause neuroleptic malignant syndrome, a rare but extremely serious reaction characterized by cardiovascular instability, decreased level of consciousness, extrapyramidal effects, and hyperpyrexia.

Monitor CBC with differential, as ordered, because drug may worsen existing blood dyscrasias, such as agranulocytosis, neutropenia, and thrombocytopenia, in patients with bone marrow suppression. Be aware that drug may worsen angleclosure glaucoma, encephalopathy, organic or traumatic brain damage, or tardive dyskinesia.

When possible, avoid combining thiethylperazine with CNS depressants because these may potentiate thiethylperazine’s effects.

Monitor patient with cardiac disease for exaggerated cardiovascular reactions.

Implement seizure precautions and monitor for seizures in patients with known seizure disorder because drug may lower seizure threshold.

Implement safety precautions, according to facility policy, for elderly patients. They may be especially sensitive to drug’s sedative and extrapyramidal effects.

Be prepared to discontinue drug 48 hours before myelography and to resume drug 24 to 48 hours afterward to minimize the risk of seizures.

Be aware that photosensitivity may turn patient’s skin yellow-brown, gray, or purple because of hyperpigmentation.

Be aware that drug shouldn’t be given to pregnant patient because it may cause jaundice and extrapyramidal symptoms in her neonate.

PATIENT SAFTY

Instruct patient to stay recumbent for 1 hour after taking thiethylperazine to minimize effects of orthostatic hypotension.

Advise patient to notify prescriber immediately about adverse CNS reactions, decreased urine output, or vision changes.

Urge patient to avoid alcohol use and potentially hazardous activities during therapy.

Encourage patient to avoid excessive sun exposure and to use sunscreen when she’s outdoors.

Advise patient on long-term therapy to have periodic eye examinations to detect possible eye disorders.

Category

Chemical class: Barbiturate
Therapeutic class: Anticonvulsant, sedativehypnotic

Pregnancy category: C

Controlled substance: Schedule III

Indications

To control seizures from anesthesia or other causes
I.V.INJECTION
Adults. Initial: 75 to 125 mg (3 to 5 ml of 2.5% solution) as soon as possible after onset of seizure. Maximum: 250 mg given over 10 min. To facilitate narcoanalysis
IV: OR INJECTION
Adults. Dosage individualized based on patient’s age, condition, sex, and weight; injected at 100 mg/min (4 ml/min of 2.5% solution) with patient counting backwards from 100. Expect to discontinue injection once patient becomes confused with her counting but is still awake. Or, use 0.2% concentration in D5W for injection and infuse at 50 ml/min. To treat cerebral hypertension
IV: OR INJECTION
Adults. 1.5 to 3.5 mg/kg, repeated as needed, to reduce elevated intracranial pressure (ICP). Route Onset Peak Duration I.V. 10–40 sec Unknown 10–30 min

Mechanism of Action

Depresses the CNS and may inhibit ascending transmission of impulses in the reticular formation. Thiopental may enhance or mimic inhibitory action of gamma-aminobutyric acid, thereby causing anticonvulsant effect and producing sedation and hypnosis. Thiopental may reduce ICP by increasing cerebral vascular resistance, which decreases cerebral blood flow and volume.

Incompatibilities

Don’t mix thiopental with acidic I.V. or solutions, succinylcholine, or tubocurarine.

Contraindications

History of porphyria; hypersensitivity to thiopental, its components, or other barbiturates

Interactions

clonidine, CNS depressants, guanabenz, magnesium sulfate, methyldopa, metyrosine, pargyline, rauwolfia alkaloids: Additive CNS depressant effects diazoxide, diuretics, guanadrel, guanethidine, mecamylamine, trimethaphan: Possibly additive hypotensive effect ketamine: Increased risk of hypotension or respiratory depression; possibly countered hypnotic effect of thiopental phenothiazines: Possibly increased CNS depression or excitation, increased hypotensive effect
alcohol use: Additive CNS depressant effects

Side Efect

CNS: Agitation, anxiety, seizures
CV: Bradycardia, hypotension, shock, tachycardia, thrombophlebitis
GI: Hiccups
RESP: Apnea, bronchospasm, cough, laryngospasm, respiratory depression, wheezing
SKIN: Hives, itching, rash, redness
Other: Angioedema

Cautions

Before administering thiopental, expect to premedicate patient with an anticholinergic, such as atropine or glycopyrrolate, to minimize secretions.

Be prepared to administer a test dose of 25 to 75 mg (1 to 3 ml of 2.5% solution) to determine tolerance or sensitivity. Expect to observe patient for at least 1 minute after administering test dose.

Dilute drug with a compatible I.V. solution before administering, such as D5W for injection, normal saline solution for injection, or sterile water for injection. Be aware that sterile water for injection shouldn’t be used to prepare 0.2% or 0.4% solution because it would result in a hypotonic solution and cause hemolysis.

To prepare 0.2% solution, dilute 1 g of thiopental with 500 ml of compatible diluent to produce a final concentration of 2 mg/ml.

To prepare 0.4% solution, dilute 1 g thiopental with 250 ml compatible diluent or 2 g thiopental with 500 ml compatible diluent to produce a final concentration of 4 mg/ml.

To prepare 2.5% solution, dilute 1 g of thiopental with 40 ml of compatible diluent or 5 g of thiopental with 200 ml of compatible diluent to produce a final concentration of 25 mg/ml.

Inspect solution for particles before administration. Use solution within 24 hours of reconstitution, and discard unused portion after 24 hours.

Monitor patient’s blood and tissue oxygenation and vital signs during I.V. administration. Keep emergency equipment and nearby in case respiratory depression occurs.

If patient has a history of CV disease or hypotension, monitor her for CV depressant effects, such as bradycardia, hypotension, or shock.

In patient with a history of seizures, institute seizure precautions according to facility protocol.

Monitor respiratory rate, rhythm, and quality for signs of respiratory depression in debilitated patient or one with a history of respiratory disease.

Monitor patient’s neurologic status every hour, or as ordered, in patient with increased ICP.

PATIENT SAFTY

Explain the need for frequent hemodynamic monitoring.

Advise patient to use caution when driving or performing tasks that require alertness for at least 24 hours after receiving thiopental.

Instruct patient not to consume alcohol or other CNS depressants for at least 24 hours after thiopental administration (unless prescribed) because they increase the effects of thiopental.

Instruct patient to report persistent drowsiness, rash, severe dizziness, or skin lesions to prescriber.

Category

Chemical class: Piperidine phenothiazine
Therapeutic class: Antipsychotic drug

Pregnancy category: Not rated

Indications

To treat schizophrenia in patients unresponsive to other antipsychotic

ORALL

, ORAL SUSPENSION, Adults and adolescents. Initial: 50 to 100 mg t.i.d., gradually increased, as needed and tolerated. Maintenance: 200 to 800 mg daily in two to four divided doses. Maximum: 800 mg daily. Children ages 2 to 12. Initial: 0.5 mg/kg daily in divided doses, gradually increased, as needed and tolerated. Maximum: 3 mg/ kg daily.

Mechanism of Action

Depresses areas of the brain that control activity and aggression, including the cerebral cortex, hypothalamus, and limbic system by blocking postsynaptic dopamine2 (D2) receptors. Drug may relieve anxiety by indirectly reducing arousal and increasing filtration of internal stimuli to the brain stem reticular activating system.

Contraindications

Coma; concurrent use of that inhibit the metabolism of thioridazine, such as fluoxetine, fluvoxamine, paroxetine, pindolol, and propranolol; concurrent use of that prolong the QT interval; concurrent use of high doses of a CNS depressant; history of arrhythmias; hypersensitivity to thioridazine, other phenothiazines, or their components; prolonged QT interval; reduced cytochrome P450 2D6 activity; severe CNS depression; severe hypertensive or hypotensive cardiac disease

Interactions

amantadine, antihistamines, antimuscarinics, clozapine, cyclobenzaprine, diphenoxylate, disopyramide, maprotilene: Additive anticholinergic effects amiodarone, bepridil, cisapride, disopyramide, erythromycin, flecainide, grepafloxacin, ibutilide, pimozide, probucol, procainamide, quinidine, sotalol, sparfloxacin, tocainide: Possibly prolonged QT interval amphetamine, chlorpromazine, dextroamphetamine: Possibly decreased effects of these and thioridazine antacids, antidiarrheals (adsorbent), kaolin, rifabutin, rifampin, rifapentine: Reduced bioavailability of thioridazine anxiolytics, benzodiazepines, clonidine, dronabinol, guanabenz, guanfacine, opioid analgesics, phenothiazines, sedative-hypnotics: Possibly increased CNS effects or hypotension barbiturates, fosphenytoin, phenytoin,
valproic acid: Increased CNS depression, lowered seizure threshold bromocriptine: Possibly decreased effectiveness of bromocriptine carbamazepine: Possibly decreased blood thioridazine level charcoal: Reduced thioridazine absorption dopamine, droperidol, haloperidol, metoclopramide, metyrosine: Possibly increased adverse CNS effects ephedrine, epinephrine, norepinephrine, phenylephrine: Possibly severe hypotension, MI, or tachycardia fluoxetine, fluvoxamine, other cytochrome P450 2D6 inhibitors, paroxetine, pindolol: Inhibited metabolism of thioridazine, leading to elevated blood thioridazine level general anesthetics: Possibly potentiated CNS depression guanadrel, guanethidine, methyldopa: Inhibited hypotensive effect of these levodopa, pergolide, pramipexole, ropinirole: Possibly inhibited antiparkinsonian response lithium (high doses): Risk of encephalopathic syndrome (characterized by confusion, elevated liver function test results and fasting blood glucose level, extrapyramidal symptoms, fever, lethargy, leukocytosis, and weakness)
MAO inhibitors: Possibly exaggerated extrapyramidal reactions methoxsalen, oral contraceptives, porfimer, sulfonamides, sulfonylureas, tetracyclines, thiazide diuretics, vitamin A analogues: Possibly increased photosensitivity propranolol: Increased blood propranolol and thioridazine levels, increased CNS effects, hypotension
tramadol: Increased blood tramadol level, possibly increased risk of seizures trazodone: Possibly additive hypotension
alcohol use: Additive CNS effects

Side Efect

CNS: Akathisia, altered temperature regulation, depression, dizziness, drowsiness, extrapyramidal reactions (dystonia, laryngospasm, motor restlessness, pseudoparkinsonism), headache, insomnia
CV: ECG changes, hypertension, hypotension, prolonged QT interval, torsades de pointes, ventricular tachycardia
EENT: Blurred vision, change in color perception, dry mouth, impaired night vision, mydriasis, photophobia
ENDO: Breast engorgement, galactorrhea
GI: Constipation, ileus, nausea
GU: Amenorrhea, decreased libido, ejaculation disorders, impotence, menstrual irregularities, priapism, urine retention
HEME: Agranulocytosis, anemia, aplastic anemia, eosinophilia, leukocytosis, leukopenia, pancytopenia, thrombocytopenia
SKIN: Hyperpigmentation, jaundice, photosensitivity
Other: Weight gain

Cautions

WARNING Expect to give thioridazine only if patient has failed to respond to therapy with at least two other antipsychotic because thioridazine may prolong the QT interval and has been associated with torsades de pointes and sudden death.
WARNING Thioridazine shouldn’t be used to treat elderly patients with dementiarelated psychosis because drug increases the risk of death in these patients.

Obtain baseline and serial ECG tracings and serum potassium levels, as ordered. Notify prescriber if QT interval is greater than 500 msec or if potassium level is abnormal, and expect to discontinue drug immediately.

Frequently monitor blood pressure and assess for chest pain in patients with heart disease because thioridazine has caused hypotension and has precipitated angina on occasion. Also monitor urine output in patients with benign prostatic hyperplasia because drug can worsen urine retention.

Be aware that high doses and large dosage changes in patient with a seizure disorder may lower seizure threshold. Institute seizure precautions, as appropriate, according to facility policy.

Administer drug with food, milk, or a full glass of water to minimize GI distress.

Measure oral suspension using calibrated measuring device. Dilute with 60 to 120 ml of fruit juice, distilled water, or acidified tap water immediately before administration.

Don’t give thioridazine oral suspension with carbamazepine oral suspension; a rubbery orange precipitate may form in stool.

To prevent contact dermatitis, don’t let oral solution come in contact with skin.

Administer antacid or adsorbent antidiarrheal at least 1 hour before or 2 hours after thioridazine.
WARNING Be aware that thioridazine can cause neuroleptic malignant syndrome— most commonly in male patients. Signs and symptoms include altered level of consciousness, altered mental status, autonomic instability (diaphoresis, hypotension or hypertension, sinus tachycardia), hyperthermia, and severe extrapyramidal dysfunction. Acute renal failure, increased serum creatine phosphokinase level, and leukocytosis also have occurred. Notify prescriber immediately if such symptoms develop, and be prepared to discontinue therapy.

Be aware that drug shouldn’t be discontinued abruptly. Sudden withdrawal of thioridazine may produce transient dizziness, nausea, tremor, and vomiting.

Assess for eye pain because drug’s anticholinergic effects can worsen angle-closure glaucoma.

Promptly investigate and report blurred vision, defective color perception, or impaired night vision because of the risk of pigmentary retinopathy.

Expect prescriber to discontinue thioridazine and order CBC if patient experiences signs of infection. Also expect drug therapy to be stopped 48 hours before myelography and resumed 24 to 48 hours afterward.

Monitor patient for signs and symptoms of tardive dyskinesia—such as uncontrollable movements of the arms, face, or legs—even after treatment stops. Notify prescriber if they develop.

PATIENT SAFTY

Instruct patient to take thioridazine exactly as prescribed and not to stop taking drug without consulting prescriber because of the risk of withdrawal symptoms.

Instruct patient to notify prescriber immediately if she develops unusual symptoms, such as dizziness, palpitations, and syncope, because they may indicate the presence of torsades de pointes.

Advise patient not to take drug within 2 hours of an antacid.

Caution patient to avoid alcohol use, which increases thioridazine’s sedative effects, and to avoid hazardous activities if drowsiness occurs.

Urge patient to notify prescriber immediately if she experiences blurred vision, defective color perception, difficulty with nighttime vision, excessive drowsiness, nausea, sore throat, or other signs of infection. Thioridazine treatment may be discontinued.

Advise female patient to use effective contraception while taking drug because its fetal effects are unknown. Instruct her to inform prescriber immediately of known or suspected pregnancy.

Because drug may alter temperature regulation, encourage patient to avoid exposure to extreme temperatures during therapy.

Advise patient to wear protective dark glasses to minimize the effects of adverse vision reactions.

If patient requires long-term therapy, explain the risk of tardive dyskinesia, and urge her to notify prescriber immediately if she develops uncontrollable movements of her arms, face, or legs.

Instruct patient to tell other prescribers that she’s taking thioridazine before she takes any new drug.

Category

Chemical class: Thioxanthene derivative
Therapeutic class: Antipsychotic

Pregnancy category: Not rated

Indications

To treat psychotic disorders, such as acute psychosis, psychotic depression, and schizophrenia (THIOTHIXENE), (THIOTHIXENE HYDROCHLORIDE) Adults and children age 12 and over. Initial: 2 mg t.i.d. (for mild conditions) or 5 mg b.i.d. (for more severe conditions), increased every wk, as needed. Usual: 10 to 40 mg daily in divided doses. Maximum: 60 mg daily (for severe conditions).
DOSAGE ADJUSTMENT For elderly patients, lowest effective dosage used for maintenance therapy; maximum dosage limited to 30 mg/ day. For some patients, one daily dose possibly used for maintenance therapy.
I.M.INJECTION(THIOTHIXENE HYDROCHLORIDE)
Adults. Initial: 4 mg b.i.d. to q.i.d. Optimal: 4 mg every 6 to 12 hr. Usual: 16 to 20 mg daily in divided doses. Maximum: 30 mg daily.

Mechanism of Action

Increases dopamine turnover by blocking postsynaptic dopamine receptors in the mesolimbic system. Eventually, dopamine neurotransmission decreases, resulting in antipsychotic effects.

Contraindications

Blood dyscrasias, coma, hypersensitivity to thiothixene or its components, Parkinson’s disease, severe CNS depression, shock, use of quinidine

Interactions

amphetamines: Decreased effectiveness of either drug antacids, antidiarrheals (adsorbent): Possibly reduced bioavailability of thiothixene antihistamines, tricyclic antidepressants: Additive anticholinergic effects, causing severe constipation, ileus, or increased intraocular pressure bromocriptine: Possibly increased serum prolactin level and decreased effectiveness of bromocriptine carbamazepine: Possibly decreased blood thiothixene level dopamine: Decreased vasoconstrictive effect of dopamine (in high doses) ephedrine, phenylephrine: Possibly reduced vasopressor response epinephrine: Possibly epinephrine reversal, leading to severe hypotension, tachycardia, and possibly MI erythromycin: Increased adverse effects of thiothixene general anesthetics, opioid analgesics, tramadol: Additive CNS effects, increased risk of seizures guanadrel, guanethidine: Possibly decreased antihypertensive effect of these hypotensive : Possibly excessive hypotension levodopa: Possibly reduced effectiveness of levodopa lithium: Possibly encephalopathic syndrome (with a blood level that exceeds 12 mEq/L)
MAO inhibitors: Possibly exaggerated extrapyramidal reactions metaraminol, methoxamine, norepinephrine: Possibly reduced vasopressor response pergolide: Possibly reduced effectiveness of pergolide propranolol: Possibly seizures and increased hypotension
quinidine: Additive orthostatic hypotension, possibly prolonged QT interval
alcohol use: Additive CNS effects, increased risk of seizures smoking: Possibly decreased blood thiothixene level

Side Efect

CNS: Agitation, akathisia, drowsiness, dystonia, fatigue, insomnia, light-headedness, neuroleptic malignant syndrome, paradoxical exacerbation of psychotic disorder, restlessness, seizures, syncope, tardive dyskinesia, weakness
CV: ECG changes, edema, hypotension, peripheral edema, tachycardia
EENT: Blurred vision, dry mouth, increased salivation, miosis, mydriasis, nasal congestion, retinopathy
ENDO: Breast engorgement, galactorrhea, hyperglycemia, hypoglycemia
GI: Anorexia, constipation, diarrhea, elevated liver function test results, ileus, increased appetite, nausea, vomiting
GU: Amenorrhea, glycosuria, impotence, priapism
HEME: Agranulocytosis, anemia, eosinophilia, hemolytic anemia, leukocytosis, leukopenia, neutropenia, pancytopenia, thrombocytopenia
SKIN: Contact dermatitis, decreased sweating, photosensitivity, pruritus, rash
Other: Hyperuricemia, weight gain

Cautions

WARNING Thiothixene shouldn’t be used to treat elderly patients with dementia-related psychosis because drug increases the risk of death in these patients.

Administer thiothixene capsules with food or milk if needed to minimize GI distress.

Don’t give drug within 1 hr of an antacid.

Dilute oral solution with 60 to 120 ml of fruit or tomato juice, milk, soup, water, or a carbonated beverage. Measure dose and administer using a calibrated measuring device. Avoid spilling solution on skin because drug may cause contact dermatitis.

Avoid inadvertent I.V. delivery of thiothixene. It’s intended for I.M. use.

Be aware that I.M. administration usually is reserved for acute, severe agitation or for patients who can’t take oral preparations.

Maintain patient in recumbent position for 30 minutes after I.M. injection to minimize orthostatic hypotension.

Assess patient for early signs of potentially irreversible tardive dyskinesia, a syndrome of involuntary rhythmic movements of the face, jaw, mouth, or tongue.
WARNING Be aware that drug can precipitate neuroleptic malignant syndrome, a serious condition characterized by altered mental status, arrhythmias, diaphoresis, hyperpyrexia, muscle rigidity, and tachycardia, especially in patients with hyperthyroidism or thyrotoxicosis. Symptoms may be severe enough to cause life-threatening respiratory depression.

Monitor patient’s serum calcium level because hypocalcemia may lead to dystonic reactions.

Keep in mind that hypotension from thiothixene may precipitate angina in patients with known cardiac disease.
WARNING Be aware that drug-induced adverse CNS reactions may mimic or suppress neurologic evidence of CNS disorders, such as brain tumor, encephalitis, encephalopathy, meningitis, Reye’s syndrome, and tetanus.

Monitor for extrapyramidal symptoms— particularly dystonias—in children with acute illnesses, including CNS infections, dehydration, gastroenteritis, measles, or varicella-zoster infections.

Monitor patient’s CBC, as ordered, because serious adverse hematologic reactions may occur, such as agranulocytosis, leukopenia, and neutropenia. More frequent monitoring during first few months of thiothixene therapy is recommended for patients with a history of druginduced leukopenia or neutropenia or who have had a significantly low WBC count in the past. If abnormalities occur during therapy, monitor patient for fever or other signs of infection, notify prescriber, and expect drug to be discontinued if abnormalities are severe.

Implement seizure precautions in patients with a history of seizures or EEG abnormalities because thiothixene can lower the seizure threshold.

Assess patient for eye pain because thiothixene’s anticholinergic effects may worsen angle-closure glaucoma. Assess patient with benign prostatic hyperplasia for urine retention.

PATIENT SAFTY

Fully inform patient facing long-term thiothixene therapy about risk of developing tardive dyskinesia.

Advise patient to avoid exposure to sunlight or ultraviolet light, and to apply sunscreen when outdoors.

Urge patient to avoid smoking or to begin a smoking cessation program while taking thiothixene.

Encourage patient to avoid extreme temperature changes during drug therapy to prevent hyperthermia or hypothermia caused by decreased sweating.

Instruct patient to immediately report sore throat or other signs of infection.

Category

Chemical class: Porcine thyroid gland hormone
Therapeutic class: Thyroid hormone replacement Pregnancy category: A

Indications

To treat hypothyroidism without myxedema Adults and children. Initial: 60 mg daily, increased by 30 mg daily every mo p.r.n. Maintenance: 60 to 120 mg daily. To treat hypothyroidism or myxedema in patients with cardiovascular disease
Adults. Initial: 15 mg daily; daily dosage doubled every 2 wk, as indicated to achieve desired response, up to 180 mg daily. Maintenance: 60 to 180 mg daily. To treat congenital hypothyroidism (cretinism) or severe hypothyroidism in children and infants Children and infants. Initial: 15 mg daily; daily dosage doubled every 2 wk, as indicated to achieve desired response, up to 180 mg daily. If desired response isn’t achieved, dosage further increased by 30 to 60 mg daily. Maintenance: Individualized.

Mechanism of Action

Stimulates growth and maturation of tissues, increases energy expenditure, and affects all enzyme actions through several mechanisms. Thyroid hormone:

regulates cell differentiation and proliferation

aids in myelination of nerves and development of axonal and dendritic processes in the nervous system

enhances protein and carbohydrate metabolism by promoting metabolic process-es that increase gluconeogenesis and protein synthesis and facilitate the mobilization of glycogen stores.

Contraindications

Acute MI not associated with hypothyroidism, hypersensitivity to thyroid USP or its components, obesity treatment, untreated thyrotoxicosis

Interactions

barbiturates, carbamazepine, phenytoin,
rifampin: Possibly increased catabolism of thyroid hormone cholestyramine, colestipol: Decreased effectiveness of thyroid hormone corticosteroids: Decreased metabolism of corticosteroids estrogens: Possibly increased circulating concentrations of thyroxine-binding globulin, decreased effectiveness of thyroid hormone insulin, oral antidiabetic : Possibly altered blood glucose control ketamine: Risk of marked hypertension and tachycardia oral anticoagulants: Altered anticoagulant effect sympathomimetics: Increased adverse cardiovascular effects tricyclic antidepressants: Increased therapeutic and toxic effects of both all : Possibly altered absorption of thyroid hormone

Side Efect

CNS: Headache, insomnia, nervousness, tremor
CV: Angina; arrhythmias, including atrial fibrillation and sinus tachycardia; palpitations
ENDO: Hyperthyroidism
GI: Diarrhea, vomiting
GU: Menstrual irregularities
SKIN: Alopecia, diaphoresis
Other: Heat intolerance, weight loss

Cautions

Avoid giving oral thyroid hormone with food because it may alter drug absorption.

Don’t give thyroid hormone within 5 hours of cholestyramine or colestipol. Giving them together can reduce hormone absorption. thyroid USP 1010
WARNING Be aware that thyroid hormone therapy can unmask or worsen adrenal insufficiency, precipitate adrenal crisis in patients with uncontrolled adrenal insufficiency, and increase the risk of arrhythmias in patients with coronary artery disease.

Monitor blood glucose level often because thyroid hormone therapy can unmask or exacerbate symptoms of other endocrine disorders and also may alter antidiabetic drug dosage requirements in patients with diabetes mellitus. Be aware that withdrawal of thyroid hormone can precipitate a hypoglycemic response in susceptible patients.

PATIENT SAFTY

Tell patient to take thyroid hormone on an empty stomach at the same time each day.

Advise her to inform prescriber immediately and seek medical attention if she experiences chest pain, nervousness, or sweating.

Instruct patient who uses cholestyramine or colestipol not to take these within 5 hours of thyroid dose.

Inform patient that full effects may not be evident for 1 to 3 weeks.

Instruct patient with diabetes mellitus to monitor blood glucose level frequently.

Category

Chemical class: Recombinant glycoprotein of human TSH
Therapeutic class: Diagnostic aid

Pregnancy category: C

Indications

To provide diagnostic follow-up of patients with well-differentiated thyroid carcinoma
I.M.INJECTION(THYROTROPIN ALFA) Adults and adolescents age 16 and over. 0.9 mg every 24 hr for 2 doses or every 72 hr for 3 doses. Scanning or serum thyroglobulin testing performed 72 hr after last injection. To provide differential diagnosis of subclinical hypothyroidism or low thyroid reserve I.M.OR SUBCUTANEOUS INJECTION (THYROTROPIN) Adults and adolescents age 16 and over. 10 international units daily for 1 to 3 days, followed by radioactive iodine study 24 hr after last injection. No response indicates thyroid failure; substantial response indicates pituitary failure. To determine thyroid status in patients receiving thyroid hormone, to differentiate between primary and secondary hypothyroidism I.M.OR SUBCUTANEOUS INJECTION (THYROTROPIN) Adults and adolescents age 16 and over. 10 international units daily for 1 to 3 days. To aid in diagnosing thyroid carcinoma remnant after surgery I.M.OR SUBCUTANEOUS INJECTION (THYROTROPIN) Adults and adolescents age 16 and over. 10 international units daily for 3 to 7 days. As adjunct for radioiodine ablation of thyroid tissue remnants in patients who have undergone a near-total or total thyroidectomy for well-differentiated thyroid cancer and who have no evidence of metastatic thyroid cancer
I.M.INJECTION(THYROTROPIN ALPHA)
Adults. 0.9 mg, followed by a second 0.9 mg 24 hours later, followed by radioiodine administration 24 hours later.

Mechanism of Action

Stimulates production of thyroglobulin by active thyroid tissue and enhances uptake of iodine, synthesis of thyroid precursor hormones (monoiodotyrosine, diiodotyrosine, and levothyroxine), and release of triiodothyronine (T3) and thyroxine (T4) from the thyroid gland into systemic circulation. Thyrotropin also binds with thyroid cancer tissue and stimulates iodine uptake in radioactive iodine imaging to detect cancer cells in euthyroid patients after neartotal or total thyroidectomy.

Contraindications

Coronary thrombosis, hypersensitivity to thyrotropin or its components, uncorrected adrenal insufficiency

Side Efect

CNS: Asthenia, fever, headache, paresthesia
ENDO: Hyperthyroidism
GI: Nausea, vomiting
RESP: Respiratory distress
SKIN: Rash, urticaria
Other: Flulike symptoms; sudden, rapid, painful enlargement of locally recurring papillary carcinoma

Cautions

WARNING Be aware that thyrotropin can unmask or worsen adrenal insufficiency, precipitate adrenal crisis in patients with uncontrolled adrenal insufficiency, and increase the risk of arrhythmias in patients with coronary artery disease.

Reconstitute thyrotropin solution with manufacturer-provided diluent, which contains no preservatives.

Administer I.M. thyrotropin injections to the buttocks.
WARNING Avoid inadvertent I.V. or intradermal injection of thyrotropin. I.V. administration may result in severe reactions, including diaphoresis, hypotension, nausea, tachycardia, and vomiting. Intradermal injection may damage tissue at injection site.

Monitor patient closely, especially during first 24 hours after drug administration, because patients have died (rarely) during this time.

Check for chest pain and increased heart rate, especially in patients with cardiac or coronary artery disease, including angina, hypertension, and recent acute MI, and in patients with residual thyroid tissue. Drug may increase serum thyroid hormone level.

PATIENT SAFTY

Advise patient to continue taking prescribed thyroid hormone replacement while receiving injections of thyrotropin alfa unless otherwise directed by prescriber.

If patient is scheduled for radioactive iodine test, tell her to follow a low-iodine diet.

Inform patient that testing may take 5 to 12 days to complete.

Category

Chemical class: Nipecotic acid derivative
Therapeutic class: Anticonvulsant

Pregnancy category: C

Indications

As adjunct to treat partial seizures
Adults. Initial: 4 mg daily; increased by 4 mg/wk up to 16 mg daily, then dosage increased by 4 to 8 mg every wk until desired response occurs. Usual: 32 to 56 mg daily. Maximum: 56 mg daily in 2 to 4 divided doses. Children ages 12 to 18. Initial: 4 mg daily for 1 wk, then increased by 4 to 8 mg/wk until desired response occurs. Maximum: 32 mg daily in 2 to 4 divided doses.
DOSAGE ADJUSTMENT For patients with impaired hepatic function, dosage individualized and reduced, or interval extended if needed, because of reduced drug clearance.

Mechanism of Action

Appears to inhibit neuronal and glial uptake of gamma-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the CNS. Tiagabine makes more GABA available in the CNS to open chloride channels in postsynaptic membranes, thereby leading to membrane hyperpolarization and preventing transmission of nerve impulses.

Contraindications

Hypersensitivity to tiagabine or its components

Interactions

benzodiazepines,
CNS depressants: Possibly additive CNS depression carbamazepine, phenobarbital,
phenytoin: Possibly decreased tiagabine effectiveness
alcohol use: Possibly additive CNS depression

Side Efect

CNS: Amnesia, anxiety, asthenia, ataxia, confusion, depression, dizziness, drowsitiagabine hydrochloride 1012 ness, EEG abnormalities, hostility, impaired cognition, insomnia, light-headedness, paresthesia, seizures, status epilepticus, suicidal ideation, tremor, weakness
EENT: Pharyngitis, stomatitis
GI: Abdominal pain, diarrhea, increased appetite, nausea, vomiting
GU: UTI
MS: Dysarthria
SKIN: Ecchymosis, rash

Cautions

Give tiagabine with food.
WARNING Expect to taper dosage gradually, as prescribed, because stopping drug abruptly may increase seizure frequency.

Take seizure precautions because tiagabine has caused seizures and status epilepticus in patients with no history of seizures.

Watch patient closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes, and report concerns at once.

PATIENT SAFTY

Instruct patient to take drug with food.

Advise patient to avoid hazardous activities until drug’s CNS effects are known. Also urge her to avoid alcohol use.

If patient takes a CNS depressant, explain that drug may increase depressant effect.

Instruct patient not to stop taking tiagabine abruptly. Explain that prescriber usually tapers dosage over 4 weeks to reduce the risk of withdrawal seizures.

Urge caregivers to watch patient closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes, and to report concerns immediately.

Category

Chemical class: Penicillin
Therapeutic class: Antibiotic

Pregnancy category: B

Indications

To treat moderate to severe infections, such as bacteremia, diabetic foot ulcers, empyema, intra-abdominal infections, lower respiratory tract infections (including pneumonia), lung abscess, peritonitis, pulmonary infections due to complications of cystic fibrosis (including bronchiectasis and pneumonia), septicemia, and skin and soft-tissue infections (including cellulitis) caused by susceptible organisms
IV: Adults and children. 200 to 300 mg/kg daily in divided doses every 4 to 6 hr. Usual: 3 g every 4 hr or 4 g every 6 hr. To treat uncomplicated UTI
IV:,
I.M.INJECTION Adults and children weighing 40 kg (88 lb) or more. 1 g every 6 hr. Children over age 1 month and weighing less than 40 kg. 50 to 100 mg/kg daily in divided doses every 6 to 8 hr. To treat complicated UTI
IV: Adults and children. 150 to 200 mg/kg in equally divided doses every 4 to 6 hr. Usual: 3 g every 6 hr.
DOSAGE ADJUSTMENT For patients with creatinine clearance of 30 to 60 ml/min/ 1.73 m2, 2 g I.V. every 4 hr; with creatinine clearance of 10 to 30 ml/min/1.73 m2, 2 g I.V. every 8 hr; with creatinine clearance of less than 10 ml/min/1.73 m2, 2 g I.V. every 12 hr or 1 g I.M. every 6 hr.

Mechanism of Action

Inhibits bacterial cell wall synthesis by binding to specific penicillin-binding proteins inside the bacterial cell wall. Ultimately, this leads to cell wall lysis and death.

Incompatibilities

Don’t administer ticarcillin through the same I.V. line as amikacin, gentamicin, or tobramycin. Don’t give within 1 hr of aminoglycosides.

Contraindications

Hypersensitivity to ticarcillin, penicillins, or their components

Interactions

aminoglycosides: Additive or synergistic activity against some bacteria, possibly mutual inactivation anticoagulants: Possibly interference with platelet aggregation, prolonged PT methotrexate: Prolonged blood methotrexate level, increased risk of methotrexate toxicity probenecid: Prolonged blood ticarcillin level

Side Efect

CV: Thrombophlebitis, vasculitis
GI: Elevated liver function test results, nausea, pseudomembranous colitis, vomiting
GU: Proteinuria
HEME: Anemia, eosinophilia, hemorrhage, leukopenia, neutropenia, prolonged bleeding time, thrombocytopenia
SKIN: Erythema nodosum, exfoliative dermatitis, pruritus, rash, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, hypernatremia, hypokalemia, injection site pain, superinfection

Cautions

Obtain body fluid or tissue samples for culture and sensitivity testing, as ordered. Review test results, if possible, before giving first dose of ticarcillin.

Don’t inject more than 2 g of drug at any one I.M. injection site.

Reconstitute each gram of ticarcillin with 4 ml of compatible diluent. Further dilute reconstituted I.V. solution to 10 to 100 mg/ml with compatible I.V. solution. To minimize vein irritation, don’t exceed concentration of 100 mg/ml. Concentrations of 50 mg/ml or greater are preferred. Infuse appropriate I.V. dose over 30 to 120 minutes.

Check for local injection site reaction, including thrombophlebitis, during therapy.

Be aware that ticarcillin may worsen symptoms in patients with a history of GI disease or colitis.

For patients with renal impairment, take seizure precautions, according to facility policy, because of increased risk of seizures.

Monitor patient closely for diarrhea, which may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold ticarcillin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Also look for signs of superinfection, such as oral candidiasis and rash in breast-feeding infant.

Monitor serum electrolyte levels for hypernatremia due to drug’s high sodium content and for hypokalemia due to increased urinary potassium loss.
WARNING Monitor patient’s platelet count, PT, and APTT because ticarcillin may increase bleeding time and, in rare cases, may induce thrombocytopenia.

PATIENT SAFTY

Stress need to take full course of ticarcillin exactly as prescribed, even if feeling better.

Urge patient to report past allergies to penicillins and to notify prescriber at once about

Side Efect

, including fever.

Advise patient to decrease sodium intake to reduce the risk of electrolyte imbalance.

Instruct patient to report diarrhea that’s severe or prolonged. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and can be serious, requiring prompt treatment.

Category

Chemical class: Thienopyridine derivative
Therapeutic class: Antithrombotic, platelet aggregation inhibitor

Pregnancy category: B

Indications

To reduce the risk of initial thrombotic stroke in patients who have experienced transient ischemic attack, to reduce the risk of recurrent stroke in patients who have previously experienced thrombotic stroke
Adults. 250 mg b.i.d. As adjunct to reduce the risk of subacute stent thrombosis after successful coronary stent implantation
Adults. 250 mg b.i.d with antiplatelet doses ticlopidine hydrochloride 1014 of aspirin for up to 30 days after successful stent implantation.

Contraindications

Coagulopathy, GI bleeding, hematologic disorders related to hematopoiesis (including history of thrombotic thrombocytopenic purpura, neutropenia, and thrombocytopenia), hemophilia, hypersensitivity to ticlopidine or its components, intracranial bleeding, retinal bleeding, severe hepatic disease

Interactions

aluminumand magnesium-containing antacids: Possibly decreased peak blood ticlopidine level antineoplastics, antithymocyte globulin, heparin, NSAIDs, oral anticoagulants, platelet aggregation inhibitors, salicylates, strontium-89 chloride, thrombolytics: Increased risk of bleeding
cimetidine: Reduced clearance of ticlopidine, increased risk of

Side Efect

cyclosporine, digoxin: Decreased blood level and possibly reduced effects of these porfimer: Decreased effectiveness of porfimer photodynamic therapy xanthines (aminophylline, oxytriphylline, theophylline): Decreased theophylline clearance, increased risk of toxicity

Side Efect

CNS: Dizziness
CV: Hypercholesterolemia, vasculitis
EENT: Tinnitus
GI: Abdominal pain, anorexia, diarrhea, elevated liver function test results, flatulence, indigestion, nausea, vomiting
HEME: Agranulocytosis, aplastic anemia, hemolysis, hemolytic anemia, neutropenia, pancytopenia, thrombocytopenia, thrombotic thrombocytopenia, thrombotic thrombocytopenic purpura
SKIN: Pruritus, purpura, rash
Other: Hyponatremia, serum sicknesslike reaction

Cautions

Give ticlopidine with food to maximize GI Ticlopidine GP IIb/IIIa receptor

Mechanism of Action

Normally, platelets don’t adhere to blood vessel walls. However, when a thrombotic stroke or other disorder damages blood vessel walls, platelets are activated and adhere within seconds. Once activated, platelets release adenosine diphosphate (ADP). This causes fibrinogen to bind to glycoprotein IIb/IIIa (GP IIb/IIIa) receptors on the surface of activated platelets and connect with other activated platelets. Then a thrombus forms. Ticlopidine inhibits the release of ADP from activated platelets, which prevents fibrinogen from binding to GP IIb/IIIa receptors on the surface of activated platelets, as shown below. This action prevents platelets from aggregating to form a thrombus, which prevents thrombosis of an implanted stent or recurrence of stroke. absorption and minimize any GI distress.

Avoid I.M. injections of other because excessive bleeding, bruising, or hematoma may occur.

During first 3 months of therapy, monitor CBC every 2 weeks, as ordered (more frequently in patients with depressed neutrophil count).

Be aware that ticlopidine therapy typically is used for patients with stroke or an increased risk of stroke who can’t tolerate aspirin because of the risk of neutropenia or agranulocytosis.
WARNING Be aware that ticlopidine therapy irreversibly affects platelet aggregation. Expect prescriber to discontinue drug 10 to 14 days before surgical procedures to prevent uncontrolled bleeding.

Monitor serum cholesterol level during first month of ticlopidine therapy for expected increase. Hypercholesterolemia may persist for duration of treatment.

PATIENT SAFTY

Urge patient to take ticlopidine with food.

Inform patient that she may be at increased risk for infection because drug may decrease WBC or platelet count, especially in first 3 months of therapy.

Advise patient to notify prescriber immediately if she has chills, fever, or sore throat.

Urge patient to keep scheduled appointments for blood tests to detect abnormalities.

Instruct patient to apply prolonged pressure to injured areas because bleeding may take longer than usual to stop. Urge her to immediately report to prescriber any unusual bleeding or bruising.

Category

Chemical class: Glycylcycline
Therapeutic class: Antibiotic

Pregnancy category: D

Indications

To treat complicated skin and skin structure infections caused by Escherichia coli, Enterococcus faecalis (vancomycin-susceptible isolates only), Staphylococcus aureus (methicillinsusceptible and -resistant isolates), Streptococcus agalactiae, Streptococcus anginosus group (includes S. anginosus, S. intermedius, and S. constellatus), Streptococcus pyogenes, and Bacteroides fragilis; to treat complicated intraabdominal infections caused by Citrobacter freundii, Enterobacter cloacae, E. coli, Klebsiella oxytoca, Klebsiella pneumoniae, Enterococcus faecalis (vancomycin-suseptible isolates only), S. aureus (methicillin-susceptible isolates only), S. anginosus group, B. fragilis, Bacteroides thetaiotaomicron, Bacteroides uniformis, Bacteroides vulgatus, Clostridium perfringens, and Peptostreptococcus micros; to treat community-acquired bacterial pneumonia caused by Streptococcus pneumoniae (penicillin-susceptible isolates), including cases with concurrent bacteremia, Haemophilus influenzae (beta-lactamase negative isolates), and Legionella pneumophila
IV:
Adults. Initial: 100 mg infused over 30 to 60 min followed by 50 mg infused over 30 to 60 min every 12 hr for 5 to 14 days for complicated skin and skin structure infections and intra-abdominal infections (7 to 14 days for community-acquired bacterial pneumonia).
DOSAGE ADJUSTMENT For patients with severe hepatic impairment, initial dosage of 100 mg should be followed by a reduced maintenance dosage of 25 mg every 12 hr.

Mechanism of Action

Inhibits protein translation in bacteria by binding to the 30S ribosomal subunit, which prevents binding of amino-acyl tRNA molecules to the ribosome complex, thus interfering with protein synthesis. Through this bacteriostatic action, bacteria are weakened.

Incompatibilities

Don’t give amphotericin B, chlorpromazine, methylprednisolone, or voriconazole simultaneously through the same Ysite.

Contraindications

Hypersensitivity to tigecycline or its components

Side Efect

CNS: Asthenia, chills, dizziness, fever, headache, insomnia, somnolence
CV: Bradycardia, hypertension, hypotension, peripheral edema, phlebitis, septic shock, tachycardia, thrombophlebitis, vasodilation
EENT: Dry mouth, taste perversion
ENDO: Hyperglycemia, hypoglycemia
GI: Abdominal pain, acute pancreatitis, anorexia, constipation, diarrhea, dyspepsia, elevated liver enzyme levels, hepatic dysfunction or failure, jaundice, nausea, pancreatitis, pseudomembranous colitis, vomiting
GU: Elevated BUN and creatinine levels, vaginal candidiasis
HEME: Anemia, increased PT, leukocytosis, thrombocythemia
MS: Back pain
RESP: Increased cough, dyspnea
SKIN: Diaphoresis, photosensitivity, pruritus, rash
Other: Anaphylaxis, hypersensitivity reaction, hypocalcemia; hypokalemia; hyponatremia; hypoproteinemia; injection site reaction, such as edema, phlebitis, inflammation, and pain

Cautions

Obtain body tissue and fluid samples for culture and sensitivity tests as ordered before giving first dose of tigecycline. Expect to begin drug therapy before test results are known.

Avoid giving tigecycline to children under age 8 because drug may cause permanent brown or yellow tooth discoloration and enamel hypoplasia.

Use tigecycline cautiously in patients hypersensitive to tetracycline antibiotics because glycylcycline antibiotics are structurally similar to tetracyclines.

Also use cautiously in patients with complicated intra-abdominal infections secondary to intestinal perforation because of the risk of septic shock.

Determine whether female patients could be pregnant before starting tigecycline therapy because the drug may cause harm to fetus.

Reconstitute each vial of tigecycline with 5.3 ml of 0.9% sodium chloride injection or 5% dextrose injection to achieve a concentration of 10 mg/ml. Note that the color will be yellow to orange. If it’s not, the solution should be discarded. Immediately withdraw reconstituted solution from the vial and add to a 100-ml I.V. bag for infusion. Drug may be stored in the I.V. bag at room temperature for up to 6 hours or refrigerated up to 24 hours before use.

If the patient’s I.V. line is used to infuse other , flush the line with either 0.9% sodium chloride injection or 5% dextrose injection before and after tigecycline infusion.

Infuse tigecycline over 30 to 60 minutes.

Monitor patient closely for diarrhea, which may indicate pseudomembranous colitis, which is known to occur with many antibiotics. If diarrhea occurs during tigecycline therapy, notify prescriber and expect to withhold drug. Expect to treat psuedomembranous colitis, if confirmed, with fluids, electrolytes, protein, and an antibiotic effective against Clostridium difficile.

Monitor patient for

Side Efect

, keeping in mind the similarity between tigecycline and tetracycline.

Assess patient for superinfection, such as vaginal candidiasis, that may result from overgrowth of nonsusceptible organisms, including fungi. If signs of infection are present, notify prescriber and provide supportive care, as prescribed.

Monitor patient’s liver function closely. If enzyme levels become elevated, notify prescriber because dosage may need to be decreased or drug discontinued.

Be aware that

Side Efect

may continue after therapy stops.

PATIENT SAFTY

Instruct patient to report adverse reactions, especially hypersensitivity reactions, such as a rash or itching, as well as diarrhea.

Tell patient to report discomfort at the infusion site because the site may need to be changed.

Urge patient to report diarrhea that’s severe or prolonged. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and can be serious, requiring prompt treatment.

Category

Chemical class: Aminobiphosphonate
Therapeutic class: Bone resorption inhibitor

Pregnancy category: C

Indications

To treat Paget’s disease in patients with serum alkaline phosphatase levels at least twice the upper limit of normal, who are symptomatic or at risk for future complications of the disease
Adults. Initial: 400 mg of tiludronic acid daily 2 hr before or after meals for 3 mo. Maximum: 400 mg of tiludronic acid daily.

Mechanism of Action

Reduces the activity of cells that cause bone loss and increases bone mass. Tiludronate may act by inhibiting osteoclast activity on newly formed bone resorption surfaces. This activity reduces the number of sites at which bone is remodeled. When bone formation exceeds bone resorption at these remodeling sites, bone mass increases. Tiludronate may also inhibit bone destruction by binding to hydroxyapatite crystals, which give bone its rigidity.

Contraindications

Creatinine clearance less than 30 ml/min/1.73 m2, esophageal abnormalities that delay esophageal emptying, hypersensitivity to tiludronate or its components

Interactions

aluminumor magnesium-containing antacids, mineral supplements (such as calcium, iron), salicylates, salicylate-containing compounds: Decreased absorption of tiludronate indomethacin: Possibly increased bioavailability of tiludronate all and beverages (except plain water): Decreased absorption of tiludronate

Side Efect

CNS: Dizziness, headache
CV: Chest pain, edema
EENT: Cataracts, conjunctivitis, glaucoma, pharyngitis, rhinitis
GI: Diarrhea, esophageal irritation and ulceration, flatulence, indigestion, nausea, vomiting
MS: Arthralgia, back pain, myalgia, osteonecrosis of jaw
RESP: Cough, upper respiratory tract infection
SKIN: Rash
Other: Flulike symptoms

Cautions

Be prepared to monitor serum calcium levels before, during, and after tiludronate therapy because drug may exacerbate such conditions as hyperparathyroidism, hypocalcemia, and vitamin D deficiency. Ensure adequate dietary intake of calcium and vitamin D during and after treatment. If hypocalcemia occurs, expect to administer a calcium supplement, as prescribed.
WARNING Be aware that tiludronate may irritate upper GI mucosa, causing such

Side Efect

as esophageal ulcer. To help minimize these reactions, have patient take drug with full glass of plain water and remain upright for at least 30 minutes.

PATIENT SAFTY

Instruct patient to take drug with 6 to 8 oz of plain water on an empty stomach (at least 2 hours before or after beverages, food, other , or mineral supplements, including mineral water) because food and beverages may severely reduce drug’s effect. Also, advise her to remain upright for at least 30 minutes after taking drug.

Advise patient not to chew or suck on tablet to reduce the risk of esophageal irritation.

Instruct patient to notify prescriber immediately if she develops signs or symptoms of esophageal irritation, such as trouble swallowing or worsening heartburn; these may indicate a serious esophageal disorder.

Caution patient not to take salicylatecontaining , such as aspirin, during tiludronate therapy.

Category

Chemical class: Beta blocker
Therapeutic class: Antihypertensive, MI prophylactic, vascular headache prophylactic

Pregnancy category: C

Indications

To manage hypertension
Adults. Initial: 10 mg b.i.d., increased every wk as prescribed. Maintenance: 20 to 40 mg daily in divided doses. Maximum: 60 mg daily. To provide long-term prophylaxis after MI
Adults. 10 mg b.i.d., beginning 1 to 4 wk after MI and continuing for at least 2 yr. To prevent migraine headache
Adults. Initial: 10 mg b.i.d. Maintenance: 20 mg daily in divided doses. Maximum: 30 mg daily; discontinued after 8 wk, as prescribed, if maximum dose is ineffective.

Mechanism of Action

Selectively blocks alpha1and beta2receptors in vascular smooth muscle and beta1 receptors in the heart. This reduces peripheral vascular resistance and blood pressure and relieves migraine headaches. Timolol’s potent beta blockade prevents the reflex tachycardia that typically occurs with most alpha blockers, and decreases cardiac excitability, cardiac output, and myocardial oxygen demand, thus preventing MI.

Contraindications

Acute bronchospasm; asthma; cardiogenic shock; children; COPD (severe); heart failure; hypersensitivity to timolol, other beta blockers, or their components; secondor third-degree AV block; severe sinus bradycardia

Interactions

allergen immunotherapy, allergenic extracts for skin testing: Increased risk of serious systemic

Side Efect

or anaphylaxis amiodarone: Additive depressant effect on cardiac conduction, negative inotropic effect anesthetics (hydrocarbon inhalation): Increased risk of myocardial depression and hypotension
beta blockers: Additive beta blockade effects calcium channel blockers, clonidine, diazoxide, guanabenz, reserpine, other hypotensionproducing : Additive hypotensive effect and, possibly, other beta blockade effects
cimetidine: Possibly interference with timolol clearance estrogens: Decreased antihypertensive effect of timolol fentanyl, fentanyl derivatives: Possibly increased risk of initial bradycardia after induction doses of fentanyl or derivative (with long-term timolol use) glucagon: Possibly blunted hyperglycemic response insulin, oral antidiabetic : Possibly masking of tachycardia in response to hypoglycemia, impaired glucose control lidocaine: Decreased lidocaine clearance, increased risk of lidocaine toxicity
MAO inhibitors: Increased risk of significant hypertension neuromuscular blockers: Possibly potentiated and prolonged action of these
NSAIDs: Possibly decreased hypotensive effect phenothiazines: Increased blood levels of both phenytoin (parenteral): Additive cardiac depressant effect sympathomimetics, xanthines: Possibly mutual inhibition of therapeutic effects

Side Efect

CNS: Asthenia, decreased concentration, depression, dizziness, fatigue, fever, hallucinations, headache, insomnia, nervousness, nightmares, paresthesia, stroke, syncope, vertigo
CV: Angina, arrhythmias, bradycardia, cardiac arrest, chest pain, edema, palpitations, Raynaud’s phenomenon, vasodilation
EENT: Diplopia, dry eyes, eye irritation, ptosis, tinnitus, vision changes
ENDO: Hyperglycemia, hypoglycemia
GI: Abdominal pain, diarrhea, hepatomegaly, indigestion, nausea, vomiting
GU: Decreased libido, impotence
MS: Arthralgia, decreased tolerance to exercise, extremity pain, muscle weakness
RESP: Bronchospasm, cough, crackles, dyspnea
SKIN: Alopecia, diaphoresis, hyperpigmentation, pruritus, purpura, rash
Other: Anaphylaxis, weight loss

Cautions

WARNING Be aware that timolol may mask evidence of acute hypoglycemia in diabetic patient. It also may mask certain signs of hyperthyroidism, such as tachycardia.

Be aware that timolol may prolong hypoglycemia by interfering with glycogenolysis or may promote hyperglycemia by decreasing tissue sensitivity to insulin.

Monitor blood pressure and cardiac output, as appropriate, for patient with a history of systolic heart failure or left ventricular dysfunction because timolol’s negative inotropic effect can depress cardiac output.
WARNING Timolol shouldn’t be discontinued abruptly because this may produce MI, myocardial ischemia, severe hypertension, or ventricular arrhythmias, particularly in patient with known cardiovascular disease.

Expect varied drug effectiveness in elderly patients; they may be less sensitive to drug’s antihypertensive effect or more sensitive because of reduced drug clearance.

Monitor for impaired circulation in elderly patients with age-related peripheral vascular disease or patients with Raynaud’s phenomenon. Such patients may experience exacerbated symptoms from increased alpha stimulation. Elderly patients also are at increased risk for beta blocker–induced hypothermia.

If timolol worsens skin condition, such as psoriasis, notify prescriber.

PATIENT SAFTY

Instruct patient taking timolol to inform prescriber of chest pain, fainting, lightheadedness, or shortness of breath, which may indicate the need for dosage change.

Caution patient not to stop taking drug abruptly. Timolol dosage must be tapered gradually under prescriber’s supervision.

Instruct patient with diabetes to monitor blood glucose level often during therapy.

Warn patient with psoriasis about possible flare-ups of skin condition.

Category

Chemical class: Synthetic nitroimidazole
Therapeutic class: Antiprotozoal

Pregnancy category: C

Indications

To treat trichomoniasis caused by Trichomonas vaginalis
Adults. 2 g one time with food. To treat giardiasis caused by Giardia duodenalis (G. lamblia)
Adults. 2 g one time with food. Children age 4 and over.50 mg/kg (up to 2 g) one time with food. To treat intestinal amebiasis caused by Entamoeba histolytica
Adults. 2 g daily for 3 days with food. Children age 4 and over.50 mg/kg (up to 2 g) daily for 3 days with food. To treat amebic liver abscess caused by Entamoeba histolytica
Adults. 2 g daily for 3 to 5 days with food. Children age 4 and over. 50 mg/kg (up to 2 g) daily for 3 to 5 days with food.
DOSAGE ADJUSTMENT For patients receiving hemodialysis, an additional dose equivalent to one-half the dose prescribed should be given after the dialysis treatment on the days dialysis is performed.

Mechanism of Action

Undergoes intracellular chemical reduction during anaerobic metabolism. After tinidazole is reduced, it damages DNA’s helical structure and breaks its strands, which inhibits bacterial nucleic acid synthesis and causes cell death.

Contraindications

Breast-feeding, hypersensitivity to tinidazole or its components, treatment of trichomoniasis during first trimester of pregnancy

Interactions

cholestyramine: Possibly decreased bioavailability of tinidazole cimetidine,
ketoconazole: Possibly delayed elimination and increased blood level of tinidazole cyclosporine, tacrolimus: Possibly increased serum cyclosporine and tacrolimus levels disulfiram: Possibly combined toxicity, resulting in confusion and psychosis fluorouracil: Possibly decreased fluorouracil clearance lithium: Possibly increased serum lithium levels oral anticoagulants: Possibly increased anticoagulant effect oxytetracycline: Possibly diminished effect of tinidazole phenobarbital, phenytoin,
rifampin: Possibly increased metabolism and decreased blood level of tinidazole
alcohol use: Possibly disulfiram-like effects

Side Efect

CNS: Ataxia, dizziness, coma, confusion, depression, drowsiness, fatigue, fever, headache, insomnia, malaise, peripheral neuropathy, seizures, vertigo, weakness
CV: Palpitations
EENT: Dry mouth, excessive salivation, furry tongue, metallic or bitter taste, oral candidiasis, pharyngitis, stomatitis, tongue discoloration
GI: Abdominal cramps, anorexia, constipation, diarrhea, epigastric discomfort, flatulence, hepatic abnormalities, indigestion, nausea, thirst, vomiting
GU: Darkened urine, dysuria, increased vaginal discharge, menorrhagia, UTI, vaginal candidiasis or odor, vulvo-vaginal discomfort
HEME: Reversible thrombocytopenia, transient leukopenia or neutropenia
MS: Arthralgia, arthritis, myalgia, pelvic pain
RESP: Bronchospasm, dyspnea, upper respiratory tract infection
SKIN: Diaphoresis, erythema multiforme, flushing, pruritus, rash, Stevens-Johnson syndrome, urticaria
Other: Angioedema

Cautions

Use tinidazole cautiously in patients with CNS disease or blood dyscrasias because tinidazole’s adverse effects may worsen these disorders. Also use cautiously in patients with hepatic impairment because a chemically related drug has reduced elimination.

Take seizure precautions. If a seizure or other abnormal neurologic symptoms occur, notify prescriber and expect to stop drug.

Treat a patient diagnosed with trichomoniasis and her sexual partner with the same dose of tinidazole and at the same time, as ordered, because trichomoniasis is a sexually transmitted disease.

Monitor patient’s total WBC count and differential if retreatment with tinidazole is needed because adverse hematologic reactions may occur with repeated use.

PATIENT SAFTY

Tell patient to take tinidazole with food to minimize gastric discomfort.

Instruct patient unable to swallow tablets to crush tinidazole and mix in artificial cherry syrup and then take with food.

Advise patient to avoid alcohol while taking tinidazole and for 3 days afterward because alcohol can cause intense flushing.

Tell patient to alert prescriber before taking tinidazole if she thinks or knows she is pregnant because tinidazole crosses the placental barrier during the first trimester and its effects on the fetus are unknown.

Instruct breast-feeding patient not to breast-feed during therapy and for 3 days after taking last dose.

Category

Chemical class: Low–molecular-weight heparin
Therapeutic class: Anticoagulant, antithrombotic

Pregnancy category: B

tinzaparin sodium 1021 T

Indications

As adjunct to treat pulmonary thromboembolism and acute symptomatic deep vein thrombosis SUBCUTANEOUS INJECTION
Adults. 175 anti-Xa international units/kg daily for at least 6 days. Maximum: 18,000 to 21,000 anti-Xa international units daily.

Mechanism of Action

Potentiates the action of antithrombin III, a coagulation inhibitor. By binding with antithrombin III, tinzaparin rapidly binds with and inactivates clotting factors (primarily fibrin and factor Xa). Without thrombin, fibrinogen can’t convert to fibrin and clots can’t form.

Contraindications

Active major bleeding; heparin-induced thrombocytopenia (current or past); hypersensitivity to tinzaparin or its components, other low–molecular-weight heparins, sulfites, benzyl alcohol, or pork products

Interactions

alteplase, anistreplase, aspirin, dextran, dipyridamole, NSAIDs, oral anticoagulants, streptokinase, sulfinpyrazone, urokinase: Possibly increased risk of bleeding and risk of spinal or epidural hematomas

Side Efect

CNS: Confusion, dizziness, epidural or spinal hematoma, headache, insomnia, intracranial hemorrhage, paralysis
CV: Angina, hypertension, hypotension, tachycardia
EENT: Epistaxis, gingival bleeding, pharyngeal bleeding
GI: Constipation, elevated liver function test results, GI and retroperitoneal bleeding, hematemesis, nausea, vomiting
GU: Hematuria, genitourinary bleeding, prolonged or heavy menstrual bleeding, UTI
HEME: Anemia, thrombocytopenia, unusual bruising
MS: Back pain
RESP: Dyspnea, hemoptysis, pulmonary embolism
SKIN: Bleeding at puncture sites, surgical incision sites, or venous cutdown sites; rash
Other: Injection site hematoma, including itching, pain, redness, and swelling

Cautions

Use tinzaparin with extreme caution in patients who are elderly and have renal insufficiency because drug may increase the risk of death.

Expect warfarin therapy to begin within 1 to 3 days of tinzaparin use.

Monitor patient’s INR. Expect therapy to continue until INR reaches 2.0 for 2 consecutive days.
WARNING Monitor patient for evidnce of GI bleeding, including bloody or black, tarry stools; bloody or coffee-ground vomitus; and severe stomach pain. Notify prescriber immediately if patient develops any of these signs or symptoms.

Assess tinzaparin injection site for signs and symptoms of hematoma, including deep, dark purple bruises under skin and itching, pain, redness, or swelling.

Assess patient for evidence of intracranial bleeding (such as decreased level of consciousness), retroperitoneal bleeding (such as abdominal pain or swelling and back pain), genitourinary bleeding (such as hematuria), or respiratory tract bleeding (such as hemoptysis). Notify prescriber immediately about any of these signs or symptoms.

If serious bleeding (not controllable by local pressure) occurs, expect to discontinue any concomitant warfarin or antiplatelet immediately.

Expect to treat bleeding by administering 1 mg of protamine sulfate 1% solution I.V. per 100 anti-Xa international units of tinzaparin, as prescribed.

If possible, avoid giving I.M. injections to patient receiving tinzaparin. If arterial puncture becomes necessary during tinzaparin therapy, expect to apply pressure after procedure and to monitor puncture site frequently for signs of bleeding.

Monitor patient’s laboratory tests for elevated liver enzyme levels. If significant elevations persist or worsen, notify prescriber immediately.
WARNING Monitor patient receiving tinzaparin and epidural or spinal anesthesia or when a spinal puncture is performed because spinal hematomas can occur, causing long-term or permanent paralysis. Watch for evidence of neurologic impairment, such as changes in sensory or motor function. If present, notify prescriber immediately because urgent care is needed to minimize effects of hematoma. Use of indwelling epidural catheters, concurent use of other that affect hemostatis, a history of traumatic or repeated epidural or spinal punctures, or a history of spinal deformity or spinal surgery increases the risk of spinal or epidural heamtomas in patients receiving tinzaparin.

PATIENT SAFTY

Advise patient who is receiving tinzaparin to immediately report any bleeding, including from nose or gums.

Instruct patient to limit physical activity during tinzaparin administration to reduce the risk of injury or bleeding.

Urge female patient to notify prescriber if she is or could be pregnant.

Category

Chemical class: Thiol compound
Therapeutic class: Antiurolithic

Pregnancy category: C

Indications

To prevent the formation of urinary cystine calculi
Adults. 800 mg daily in 3 divided doses. Children over age 9. 15 mg/kg in 3 divided doses.
DOSAGE ADJUSTMENT For patients with a history of hypersensitivity to penicillamine, therapy initiated at a reduced dosage; later dosage adjusted as prescribed, according to urine cystine level.

Mechanism of Action

Inhibits the formation of urinary cystine calculi by undergoing thiol-disulfide exchange with cystine (cystine-cystine disulfide) to form a water-soluble compound, tiopronin-cystine disulfide.

Contraindications

History of agranulocytosis, aplastic anemia, or thrombocytopenia; hypersensitivity to tiopronin or its components

Interactions

bone marrow depressants: Increased risk of adverse hematologic effects hepatotoxic : Increased risk of hepatotoxic effects nephrotoxic : Increased risk of nephrotoxic effects

Side Efect

CNS: Chills, fever
CV: Peripheral edema
EENT: Laryngeal edema, stomatitis
GU: Hematuria, proteinuria
HEME: Anemia, eosinophilia, leukopenia, thrombocytopenia
MS: Arthralgia
SKIN: Ecchymosis, jaundice, pruritus, rash, urticaria

Cautions

Watch for drug fever, which may occur during first month of tiopronin therapy.

Be aware that drug may be stopped temporarily, then restarted at lower dose.

Expect to monitor urine cystine level so dosage can be adjusted to keep cystine level below 250 g/ml.

PATIENT SAFTY

Instruct patient to take tiopronin on an empty stomach, 1 hour before or 2 hours after meals, for faster drug absorption.

Advise patient to drink at least 3 L of fluid daily to maintain a urine output of at least 2 L daily during therapy.

Urge patient to maintain a diet low in methionine, which is an essential amino acid found in eggs, cheese, fish, and milk.

Category

Chemical class: Nonane bromide monohydrate
Therapeutic class: Anticholingeric, bronchodilator

Pregnancy category: C

Indications

To prevent bronchospasm associated with COPD, including chronic bronchitis and emphysema; to reduce COPD exacerbations AEROSOL
Adults. 18 mcg (1 capsule) with 2 inhalations once daily using HandiHaler inhalation device

Mechanism of Action

Prevents acetylcholine from attaching to muscarinic receptors on membranes of smooth-muscle cells. By blocking acetylcholine’s effects in the bronchi and bronchioles, tiotropium relaxes smooth muscles and causes bronchodilation.

Contraindications

Hypersensitivity to atropine or its derivatives, including ipratropium, tiotropium, or their components

Interactions

anticholinergics: Possibly increased anticholinergic effects

Side Efect

CNS: Depression, difficulty speaking, dizziness, paresthesia, stroke
CV: Angina, atrial fibrillation, chest pain, hypercholesterolemia, palpitations, peripheral edema, supraventricular tachycardia, tachycardia
EENT: Applicaiton site irritation (glossitis, mouth ulceration, pharyngolaryngeal pain), blurred vision, cataract, dry mouth, epistaxis, eye pain, glaucoma, hoarseness, laryngitis, oral candidiasis, pharyngitis, rhinitis, sinusitis, stomatitis, throat irritation, visual halos
ENDO: Hyperglycemia
GI: Abdominal pain, constipation, dysphagia, gastroesophageal reflux, indigestion, intestinal obstruction, ileus, vomiting
GU: Urinary difficulty, urine retention, UTI
MS: Arthritis, leg or skeletal pain, myalgia
RESP: Cough, paradoxical bronchospasm, upper respiratory tract infection
SKIN: Pruritus, rash, urticaria
Other: Allergic reaction, angioedema, candidiasis, flulike symptoms, infection

Cautions

Use tiotropium cautiously in patients with angle-closure glaucoma, benign prostatic hyperplasia, or bladder neck obstruction.
WARNING Monitor patient closely after giving first dose of tiotropium for immediate hypersensitivity reactions, including angioedema and paradoxical bronchospasm. If reaction occurs, notify prescriber and expect to stop tiotropium and provide supportive care. Because atropine is of a similar structure, monitor patients hypersensitive to atropine closely when giving tiotropium because of potential for similar hypersensitivity reactions. Also use tiotropium cautiously in patients who have severe hypersensitivity to milk proteins.

Monitor patient’s renal function, as ordered, especially in patients with moderate to severe renal impairment, because tiotropium is excreted mainly by the kidneys.

Monitor patient’s pulmonary function, as ordered, to evaluate the effectiveness of tio-tropium.

PATIENT SAFTY

Caution patient not to use tiotropium to treat acute bronchospasm.

Instruct patient on the proper use of the HandiHaler inhalation device. Tell patient to place the capsule into the center chamber of the inhalation device and then to press and release the button on the side of the inhalation device to pierce the capsule. Then have the patient exhale completely, close her lips around the mouthpiece, inhale slowly and deeply, and hold her breath for as long as is comfortable.

Alert patient that the HandiHaler device should not be used for taking any other drug and that tiotropium must be taken only using the device and never swallowed.

Tell patient not to expose capsules to air until ready for use. To remove a capsule from the blister pack, tell patient to open the foil only as far as the stop line to avoid exposing the rest of the capsules in the blister pack to air. Instruct patient to discard capsules if they are inadvertently exposed to air and won’t be used immediately.

Advise patient to keep powder out of her eyes because it may irritate them or blur her vision.

Instruct patient to rinse her mouth after each treatment to help minimize throat dryness and irritation.

Advise patient to tell prescriber about decreased response to tiotropium as well as difficulty urinating, eye pain, palpitations, and vision changes.

Category

Chemical class: Tyrosine derivative
Therapeutic class: Platelet aggregation inhibitor

Pregnancy category: B

Indications

To treat acute coronary syndrome
IV:
Adults. 0.4 mcg/kg/min for 30 min, followed by 0.1 mcg/kg/min.
DOSAGE ADJUSTMENT For patients with creatinine clearance of less than 30 ml/min/ 1.73 m2, infusion rate reduced by one-half.

Mechanism of Action

Binds to glycoprotein IIb/IIIa receptor sites on the surface of activated platelets. Circulating fibrinogen can bind to these receptor sites and link platelets together, forming a clot that eventually blocks a coronary artery. By binding to receptor sites, tirofiban prevents the normal binding of fibrinogen and other factors and inhibits platelet aggregation.

Incompatibilities

Don’t infuse tirofiban in same I.V. line with any drug other than atropine sulfate, dobutamine, dopamine, epinephrine hydrochloride, furosemide, heparin, lidocaine, midazolam hydrochloride, morphine sulfate, nitroglycerin, potassium chloride, propranolol hydrochloride, or famotidine (Pepcid injection).

Contraindications

Acute pericarditis; arteriovenous malformation; coagulopathy; stroke that occurred within previous 30 days or a history of hemorrhagic stroke; GI or GU bleeding; hemophilia; history of thrombocytopenia after tirofiban use; hypersensitivity to tirofiban or its components; intracranial aneurysm or mass, intracranial bleeding, retinal bleeding, aortic dissection, or any evidence of active abnormal bleeding within previous 30 days; major surgery or trauma within previous 6 weeks; severe uncontrolled hypertension (systolic blood pressure above 180 mm Hg, diastolic blood pressure above 110 mm Hg)

Interactions

antineoplastics, antithymocyte globulin, NSAIDs, oral anticoagulants, platelet aggregation inhibitors, strontium-89 chloride, thrombolytics: Increased risk of bleeding levothyroxine, omeprazole: Increased rate of tirofiban clearance porfimer: Decreased effectiveness of porfimer photodynamic therapy salicylates: Increased risk of bleeding, possibly hypoprothrombinemia

Side Efect

CNS: Chills, dizziness, fever, headache, intracranial hemorrhage
CV: Edema, hemopericardium, peripheral edema, sinus bradycardia
GI: Hematemesis, nausea, retroperitoneal bleeding, vomiting
GU: Hematuria, pelvic pain
HEME: Severe thrombocytopenia with chills, fever, and possibly fatal bleeding complications
RESP: Pulmonary hemorrhage
SKIN: Diaphoresis, rash, urticaria
Other: Allergic reaction, anaphylaxis, infusion site bleeding

Cautions

WARNING Dilute 50-ml vial of tirofiban before use; don’t dilute 500-ml container because it holds premixed solution ready for I.V. infusion. Don’t use solution unless it’s clear and the seal is intact.

If prescribed, give tirofiban with heparin for 48 to 108 hours. Expect to continue infusion throughout angiography and for 12 to 24 hours after angioplasty or atherectomy.
WARNING If patient is also receiving a heparin infusion, expect to monitor APTT before treatment, 6 hours after heparin infusion starts, and regularly thereafter. Expect to adjust heparin dosage to maintain APTT at about two times the control. Notify prescriber immediately if patient develops an abnormally high APTT. Also, assess patient for signs and symptoms of abnormal bleeding and report them to prescriber immediately because potentially life-threatening bleeding may occur.

After cardiac catheterization or percutaneous transluminal coronary angioplasty, keep patient on bed rest with head of bed elevated. Ensure hemostasis of percutaneous site for at least 4 hours before discharge. Minimize invasive procedures, including epidural procedures, to reduce the risk of bleeding.

Monitor patient’s platelet count, hemoglobin level, and hematocrit, as ordered. Expect to discontinue tirofiban if patient’s platelet count is less than 90,000/mm3. Expect to give a platelet transfusion, as prescribed, if platelet count falls below 50,000/mm3.

PATIENT SAFTY

Advise patient to immediately report any bleeding, bruising, headache, pain, or swelling during I.V. infusion of tirofiban.

Category

Chemical class: Imidazoline
Therapeutic class: Antispasmodic

Pregnancy category: C

Indications

To manage acute and intermittent increases of muscle tone with spasticity
Adults. 4 mg every 6 to 8 hr, p.r.n., increased gradually by 2 to 4 mg/dose, as needed and as prescribed. Maximum: 36 mg daily or 3 doses daily.

Mechanism of Action

Reduces spasticity by decreasing the release of excitatory amino acids. This alpha2adrenergic agonist’s action increases presynaptic inhibition of spinal motor neurons, with the greatest effects on polysynaptic pathways.

Contraindications

Hypersensitivity to tizanidine or its components, use with ciprofloxacin or fluvoxamine

Interactions

acetaminophen: Delayed peak effects of acetaminophen alpha2-adrenergic agonists: Possibly significant hypotension antihypertensives: Additive hypotensive effects CYP1A2 inhibitors (such as acyclovir, amiodarone, cimetidine, famotidine, mexiletine, propafenone, ticlopidine, verapamil, zileuton), fluroquinolones (including ciprofloxacin, fluvoxamine): Possibly increased plasma tizanidine level; increased risk of hypotension and sedation oral contraceptives: Decreased tizanidine clearance rofecoxib: Possibly increased adverse reactions
alcohol use: Increased adverse effects of tizanidine, additive CNS depression

Side Efect

CNS: Anxiety, delusions, drowsiness, dyskinesia, fatigue, fever, hallucinations, slurred speech
CV: Orthostatic hypotension
EENT: Dry mouth, pharyngitis, rhinitis
GI: Abdominal pain, anorexia, constipation, diarrhea, dyspepsia, elevated liver function test results, hepatic failure, hepatomegaly, nausea, vomiting
GU: Urinary frequency, UTI
MS: Back pain, muscle weakness, myasthenia
SKIN: Diaphoresis, jaundice, rash, ulceration tizanidine hydrochloride 1026

Cautions

Be aware that extreme caution is required if tizanidine is prescribed for a patient with hepatic impairment because the drug is extensively metabolized in the liver.

Monitor hepatic and renal function for first 6 months and periodically thereafter.

Expect prolonged drug use to inhibit saliva.

Be aware that tizanidine should be stopped slowly to prevent withdrawal and rebound hypertension, tachycardia, and hypertonia.

PATIENT SAFTY

Caution patient not to stop taking tizanidine suddenly to prevent adverse effects.

Advise patient to change positions slowly to minimize effects of orthostatic hypotension.

Urge patient to avoid alcohol during drug therapy because of its additive CNS effects.

Tell patient to notify prescriber or a dentist if dry mouth lasts longer than 2 weeks.

Instruct patient to inform all prescribers and pharmacists about any drug he starts or stops taking.

Category

Chemical class: Aminoglycoside
Therapeutic class: Antibiotic

Pregnancy category: D

Indications

To treat bacteremia; bone and joint, gynecologic, intra-abdominal, lower respiratory tract, skin and soft-tissue, and urinary tract infections; endocarditis; meningitis; neonatal sepsis; pyelonephritis; and septicemia caused by susceptible strains of Acinetobacter species, Aeromonas species, Citrobacter species, Enterobacter species, Escherichia coli, Haemophilus influenzae (beta lactamase–negative and –positive), Klebsiella species, Morganella morganii, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Pseudomonas aeruginosa, Salmonella species, Serratia species, Shigella species, Staphylococcus aureus, and Staphylococcus epidermidis; to treat febrile neutropenia
IV:,
I.M.INJECTION
Adults. 3 to 6 mg/kg daily in divided doses every 8 to 12 hr. Children over age 5. 2 to 2.5 mg/kg every 8 hr. Children under age 5. 2.5 mg/kg every 8 to 16 hr. Neonates over age 7 days weighing more than 2 kg (4.4 lb). 2.5 mg/kg every 8 hr. Neonates over age 7 days weighing 1.2 to 2 kg (2.6 to 4.4 lb). 2.5 mg/kg every 8 to 12 hr. Neonates age 7 days and under weighing 2 kg or more.2.5 mg/kg every 12 hr. Neonates age 7 days and under weighing 1.2 to 2 kg. 2.5 mg/kg every 12 to 18 hr. Preterm neonates weighing 1 to 1.2 kg (2.2 to 2.6 lb). 2.5 mg/kg every 18 to 24 hr. Preterm neonates weighing less than 1 kg. 3.5 mg/kg every 24 hr. To treat pulmonary infection caused by P. aeruginosa in patients with cystic fibrosis
IV: Adults and children. 2.5 to 3.3 mg/kg every 8 hr; dosage adjusted to achieve peak blood drug level of 8 to 12 mcg/ml and trough blood drug level below 2 mcg/ml. INHALATION Adults and children over age 6. 1 ampule (300 mg) b.i.d. in alternating periods of 28 days on and 28 days off. To treat meningitis caused by susceptible organisms

INTRATHECAL

INJECTION
Adults. 4 to 8 mg daily with parenteral therapy. Children. 1 to 2 mg daily with parenteral therapy. To treat systemic infection INTRAPERITONEAL INFUSION Adults and children. 1.5 to 2 mg/kg. To treat dialysis-associated peritonitis in patients with end-stage renal disease INTRAPERITONEAL INFUSION Adults and children. 4 to 8 mg/L in each dialysate exchange bag, increased, as prescribed, to 6 to 8 mg/L in documented Pseudomonas infection or to 20 mg/L administered in one exchange bag daily.
DOSAGE ADJUSTMENT For patients with renal impairment, dosage possibly reduced.

Mechanism of Action

Inhibits bacterial protein synthesis by binding irreversibly to one of two aminoglycoside-binding sites on the 30S ribosomal subunit, resulting in bacteriostatic effects. Bactericidal effects may stem from tobramycin’s ability to accumulate within cells so that the intracellular drug level exceeds the extracellular level.

Incompatibilities

Don’t mix tobramycin in same solution with parenteral aminoglycosides or betalactam antibiotics because mutual inactivation may result. Don’t dilute or mix inhalation solution in nebulizer with dornase alfa.

Contraindications

Concurrent cidofovir therapy; hypersensitivity to tobramycin, aminoglycosides, sodium bisulfite, or their components

Interactions

acyclovir, aminoglycosides, amphotericin B, carboplatin, cisplatin, NSAIDs, vancomycin: Additive nephrotoxicity carbenicillin, ticarcillin: Possibly inactivation of tobramycin dimenhydrinate: Possibly masking of symptoms of ototoxicity ethacrynic acid, furosemide: Additive ototoxicity general anesthetics, neuromuscular blockers: Possibly increased neuromuscular blockade

Side Efect

CNS: Confusion, dizziness, headache, lethargy, neurotoxicity, vertigo
EENT: Hearing loss, tinnitus
GI: Clostridium difficile–associated diarrhea, diarrhea, elevated liver function test results, nausea, vomiting
GU: Elevated BUN and serum creatinine levels, nephrotoxicity, oliguria, proteinuria, renal failure
HEME: Anemia, leukocytosis, leukopenia, neutropenia, thrombocytopenia
SKIN: Exfoliative dermatitis, pruritus, rash, urticaria
Other: Hypocalcemia, hypokalemia, hypomagnesemia, hyponatremia, injection site pain

Cautions

Obtain fluid and tissue samples for culture and sensitivity testing before and during tobramycin therapy, as ordered. Review results, if available, before therapy starts.

After reconstituting with 30 ml of sterile or bacteriostatic water for injection, dilute further with normal saline solution or D5W.

Give each I.V. dose over 20 to 60 minutes.
WARNING Don’t infuse tobramycin over less than 20 minutes to avoid neuromuscular blockade and excessive peak drug level.

Don’t expose ampules for inhalation solution to intense light. Refrigerate them at 36° to 46° F (2° to 8° C).

Because drug can cause bilateral and irreversible hearing loss, assess for early signs of cochlear and vestibular ototoxicity, including high-frequency hearing loss and vertigo.

Monitor serum calcium, magnesium, potassium, and sodium levels to detect electrolyte imbalances.
WARNING Be alert for allergic reactions, including anaphylaxis, because some forms of drug contain sodium bisulfite.

Stop tobramycin therapy 7 days before starting cidofovir therapy, as prescribed.

Watch for signs of nephrotoxicity, such as elevated BUN and serum creatinine levels.

Expect dehydration to increase the risk of nephrotoxicity.
WARNING Monitor patient with myasthenia gravis or parkinsonism for increased muscle weakness because of tobramycin’s potential curare-like effect.

Monitor patient closely for diarrhea, which may indicate pseudomembranous colitis caused by C. difficile. If diarrhea occurs, notify prescriber, expect to withhold tobramycin, and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

PATIENT SAFTY

For inhaled tobramycin, instruct patient to inhale over 10 to 15 minutes, using a handheld nebulizer with a compressor.

Teach patient how to use nebulizer while sitting or standing upright and to breathe normally through its mouthpiece. Nose clips may help patient breathe through her mouth.

Instruct patient to disinfect her nebulizer every other treatment day by boiling the nebulizer parts (except tubing) for a full 10 minutes and then drying the parts on a clean, lint-free cloth.

Urge patient to immediately report highfrequency hearing loss and vertigo.

Instruct female patient to notify prescriber immediately about known or suspected pregnancy because drug poses danger to fetus.

Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools may occur 2 or more months after antibiotic therapy and may be serious, requiring prompt treatment.

Category

Chemical class: Lidocaine analogue
Therapeutic class: Class IB antiarrhythmic

Pregnancy category: C

Indications

To treat life-threatening, sustained ventricular tachycardia
Adults. Initial: 400 mg every 8 hr. Maintenance: 1.2 to 1.8 g daily in divided doses every 8 hr.
DOSAGE ADJUSTMENT Dosage possibly reduced by 25% if creatinine clearance is 10 to 30 ml/min/1.73 m2and by 50% if creatinine clearance is less than 10 ml/min/ 1.73 m2.

Mechanism of Action

Combines with fast sodium channels in myocardial cell membranes, which inhibits sodium influx into cells and decreases ventricular depolarization, automaticity, and excitability during diastole.

Contraindications

Hypersensitivity to tocainide or its components, secondor third-degree AV block without ventricular pacemaker

Interactions

antiarrhythmics: Possibly additive cardiac effects, additive toxicity
beta blockers: Increased cardiac index, left ventricular pressures, and pulmonary artery wedge pressures
cimetidine: Possibly decreased blood tocainide level
rifampin: Accelerated hepatic metabolism of tocainide, reduced tocainide effectiveness

Side Efect

CNS: Agitation, anxiety, ataxia, coma, confusion, depression, dizziness, fatigue, hallucinations, headache, mood changes, nervousness, paresthesia, psychosis, seizures, sleep disturbance, syncope, tremor, vertigo
CV: AV conduction disorders, bradycardia, chest pain, heart failure, hypertension, hypotension, palpitations, prolonged QT interval, PVCs, tachycardia, ventricular fibrillation
EENT: Blurred vision, vision changes
GI: Anorexia, diarrhea, nausea, vomiting
HEME: Agranulocytosis, anemia, aplastic anemia, bone marrow depression, hemolysis, leukopenia, neutropenia, thrombocytopenia
RESP: Pulmonary edema, fibrosis, and hypersensitivity (pneumonitis); respiratory arrest
SKIN: Diaphoresis, exfoliative dermatitis, pruritus, rash, skin lesions, urticaria

Cautions

Monitor CBC with differential weekly during first 3 months of tocainide treatment and routinely thereafter to detect blood dyscrasias. Although rare, agranulocytosis, anemia, aplastic anemia, bone marrow depression, hemolysis, leukopenia, neutropenia, or thrombocytopenia may be fatal. Expect findings to normalize about 1 month after therapy stops.

Maintain continuous cardiac monitoring or obtain periodic ECG tracings, as ordered, to assess drug effectiveness.

Watch for tremor, a possible sign of maximum dosing.

Assess patient for additive adverse cardiac effects, especially if tocainide is used with another antiarrhythmic.

Be aware that tocainide is secreted in breast milk and has the potential to cause serious

Side Efect

in breast-feeding infants.

PATIENT SAFTY

Inform patient that electrophysiologic studies may be performed before tocainide therapy starts.

Tell patient to notify prescriber about tremor because dosage may need adjustment.

Explain that chest X-rays may be needed if adverse pulmonary reactions occur.

Inform patient that ambulatory monitoring may be needed to verify antiarrhythmic response.

Stress the importance of keeping all scheduled appointments for follow-up blood tests.

Category

Chemical class: Recombinant human antihuman interleukin 6 (IL-6) monoclonal antibody
Therapeutic class: Biologic disease-modifying antirheumatic drug (DMARD)

Pregnancy category: C

Indications

To treat moderate to severe active rheumatoid arthritis in patients who have had an inadequate response to one or more tumor necrosis factor antagonist therapies
IV:
Adults. 4 mg/kg given over 60 minutes every 4 wk, increased, as needed, to 8 mg/ kg given over 60 minutes every 4 wk. Maximum: 800 mg per infusion.
DOSAGE ADJUSTMENT Dosage reduced from 8 mg/kg to 4 mg/kg for management of dose-related laboratory changes, including elevated liver enzymes (AST or ALT 1 to 3 times the upper limit of normal), neutropenia (absolute neutrophil count approaching 1,000/mm3), or thrombocytopenia (platelet count approaching 100,000/mm3).

Mechanism of Action

Binds to interleukin 6 (IL-6) receptors to interrupt signaling through them. IL-6 is a proinflammatory cytokine produced by various cells, such as Tand B-cells, lymphocytes, monocytes, and fibroblasts. It also is produced by synovial and endothelial cells, leading to local production of IL-6 in joints affected by inflammatory processes such as rheumatoid arthritis. Binding of IL-6 receptors prevents inflammationrelated signals from being relayed, which reduces inflammatory response and relieves signs and symptoms of rheumatoid arthritis.

Incompatabilities

Don’t mix tocilizumab with other .

Contraindications

Hypersensitivity to tocilizumab or its components, absolute neutrophil count below 2,000/mm3, platelet count below 100,000/mm3, ALT or AST above 1.5 times upper limit of normal

Interactions

anti-CD20 monoclonal antibodies, IL-1R antagonists, selective co-stimulation modulators, TNF antagonists: Increased risk of immunosuppression and infection atorvastatin; cytochrome P-450 substrates with a narrow therapeutic index such as cyclosporine, theophylline, warfarin; CYP3A4 substrates such as lovastatin, oral contraceptives, simvastain; omeprazole: Possibly decreased plasma levels of these with decreased effectiveness live vaccines: Increased risk of adverse vaccine effects

Side Efect

CNS: Dizziness, headache
CV: Elevated lipid levels, hypertension
EENT: Nasopharyngitis, oral ulceration
GI: Diverticulitis, elevated liver enzymes, gastritis, gastroenteritis, perforation, upper abdominal pain
GU: UTI
HEME: Neutropenia, thrombocytopenia
MS: Bacterial arthritis
RESP: Bronchitis, pneumonia, upper respiratory tract infection
SKIN: Cellulitis, pruritus, rash, urticaria
Other: Anaphylaxis, anti-tocilizumab antibodies, herpes zoster, malignancies, opportunistic infections including activation of latent infections, sepsis, tuberculosis with pulmonary or extrapulmonary disease

Cautions

Tocilizumab may be used as monotherapy to treat rheumatoid arthritis or together with methotrexate or other nonbiological DMARDs.

Tocilizumab isn’t recommended for patients with active liver disease or impairment because drug may adversely affect liver function.

Make sure patient has a tuberculin skin test before therapy starts. If skin test is positive, tuberculosis treatment will need to be started before tocilizumab therapy can begin. Even patients who have tested negative for tuberculosis may develop tuberculosis during therapy. Monitor patient for persistent cough, wasting or weight loss, and low-grade fever and report such findings to prescriber.
WARNING If patient has evidence of an active infection when drug is prescribed, therapy shouldn’t start until infection has been treated. Monitor all patients for infections, including invasive fungal infections such as aspergillosis, candidiasis, or pneumocystis; or bacterial, myobacterial, protozoal, or viral opportunistic infections during and after therapy, especially patients who are taking immunosuppressants. If a serious infection develops, expect prescriber to interrupt drug therapy until infection is controlled.

Obtain a baseline of patient’s absolute neutrophil count, platelet count, and liver enzymes before starting tocilizumab therapy, as ordered. Therapy shouldn’t begin if patient’s absolute neutrophil count is below 2,000/mm3, platelet count below 100,000/mm3or ALT or AST level is above 1.5 times the upper limit of normal. Monitor these values, as ordered, every 4 to 8 weeks and report abnormalities.
DOSAGE ADJUSTMENT may be required or drug may need to be discontinued.

Use tocilizumab cautiously in patients with recurrent infection or increased risk of infection, patients who live in regions where tuberculosis and histoplasmosis are endemic, and patients with a history of CNS demyelinating disorders because they may occur, although rarely, during tocilizumab therapy.

When preparing to give tocilizumab, begin by withdrawing from a 100-ml infusion bag or bottle containing 0.9% sodium chloride injection a volume equal to the volume of tocilizumab solution in the patient’s dose. Slowly add drug from each vial into infusion bag or bottle and gently invert bag to mix while avoiding foaming. Discard any unused drug left in vials. Once fully diluted, solution may be stored in the refrigerator or at room temperature for up to 24 hours.

Give tocilizumab with an infusion set, and never as I.V. push or bolus. Don’t infuse concurrently with other in same I.V. line.
WARNING Stop tocilizumab immediately and notify prescriber if patient has an allergic reaction. Provide supportive care, as needed.

PATIENT SAFTY

Review the signs and symptoms of an allergic reaction (rash, swollen face, difficulty breathing), and tell patient to seek emergency care immediately if these occur.

Inform patient that infections, including activation of latent infections such as tuberculosis, may occur during tocilizumab therapy. Instruct him to report unusual, persistent, or severe signs and symptoms to prescriber.

Instruct patient to immediately contact a healthcare provider about severe, persistant abdominal pain because it could reflect GI perforation.

Advise patient to avoid people with infections and to have all prescribed laboratory tests performed.

Inform patient that risk of developing a malignancy is higher in patients taking tocilizumab but is still rare. Emphasize importance of follow-up visits and reporting any unusual or sudden signs or symptoms.

Category

Chemical class: First-generation sulfonylurea
Therapeutic class: Antidiabetic

Pregnancy category: C

Indications

As adjunct to treat type 2 diabetes mellitus that’s uncontrolled by diet and exercise
Adults. Initial: 100 mg daily with breakfast if fasting blood glucose level is less than 200 mg/dl; 250 mg daily if fasting blood glucose level is more than 200 mg/dl. Dose adjusted every wk by 100 to 250 mg, if needed. Doses greater than 500 mg daily are divided and given every 12 hr. Maximum: 1,000 mg daily.
DOSAGE ADJUSTMENT If patient takes more than 40 units daily of insulin, initial dosage increased to 250 mg daily and insulin dosage decreased by 50%.

Mechanism of Action

Stimulates insulin release from beta cells in the pancreas. Tolazamide also increases peripheral tissue sensitivity to insulin either by enhancing insulin binding to cellular receptors or by increasing the number of insulin receptors.

Contraindications

Diabetic coma; diabetic ketoacidosis; hypersensitivity to tolazamide, sulfonylureas, or their components; pregnancy; sole therapy for type 1 diabetes mellitus

Interactions

ACE inhibitors, anabolic steroids, androgens, azole antifungals, bromocriptine, chloramphenicol, clofibrate, disopyramide, guanethidine, H2-receptor antagonists, insulin, magnesium salts, MAO inhibitors, methyldopa, octreotide, oxyphenbutazone, phenylbutazone, probenecid, quinidine, salicylates, sulfonamides, tetracycline, theophylline, tricyclic antidepressants, urinary acidifiers: Increased risk of hypoglycemia asparaginase, calcium channel blockers, cholestyramine, clonidine, corticosteroids, danazol, diazoxide, estrogen, glucagon, hydantoins, isoniazid, lithium, morphine, nicotinic acid, oral contraceptives, phenothiazines, rifabutin, rifampin, sympathomimetics, thiazide diuretics, thyroid , urinary alkalizers: Increased risk of hyperglycemia
beta blockers: Possibly hyperglycemia or masking of signs and symptoms of hypoglycemia digoxin: Increased risk of digitalis toxicity pentamidine: Initial hypoglycemia and then hyperglycemia if beta cell damage occurs
alcohol use: Altered blood glucose control (usually hypoglycemia), possibly disulfiram-like reaction

Side Efect

CNS: Dizziness, fatigue, headache, malaise, paresthesia, vertigo
ENDO: Hypoglycemia
GI: Anorexia, cholestasis, heartburn, nausea, vomiting
HEME: Agranulocytosis, aplastic anemia, hemolysis, hemolytic anemia, leukopenia, thrombocytopenia
MS: Muscle weakness
SKIN: Erythema, photosensitivity, pruritus, rash, urticaria

Cautions

When switching an insulin-treated patient with type 2 diabetes, expect to start tolazamide at 100 mg daily if patient takes less than 20 units daily of insulin, or 250 mg daily if patient takes 20 to 40 units daily of insulin.

Anticipate that patient receiving tolazamide may need temporary insulin treatment during periods of physiologic stress, such as fever, surgery, systemic infection, and trauma.

For patient over age 65, expect to start tolazamide at 100 mg daily.

Assess elderly patients for signs of hypoglycemia because they’re more susceptible to drug’s hypoglycemic effect. Anticipate that hypoglycemia may be more difficult to detect.

Assess patient with thyroid disease for altered blood glucose control because thyroid hormone increases GI absorption of glucose.

Expect prescriber to stop tolazamide 2 weeks before pregnant patient delivers her neonate to minimize the risk of prolonged hypoglycemia in neonate.

PATIENT SAFTY

Advise patient to avoid alcohol while taking tolazamide.

Teach patient and family members how to monitor blood glucose level and how to recognize signs of hypoglycemia and hyperglycemia.

Instruct patient to treat mild hypoglycemia with fruit juice or other simple sugars.

Category

Chemical class: First-generation sulfonylurea
Therapeutic class: Antidiabetic

Pregnancy category: C

Indications

As adjunct to treat type 2 diabetes mellitus that’s uncontrolled by diet and exercise
Adults. Initial: 1 to 2 g daily in divided doses b.i.d. or t.i.d. Maintenance: 0.25 to 2 g daily. Maximum: 3 g daily.

Mechanism of Action

Stimulates insulin release from beta cells in the pancreas. Tolbutamide also increases peripheral tissue sensitivity to insulin either by enhancing insulin binding to cellular receptors or by increasing the number of insulin receptors.

Contraindications

Diabetes complicated by pregnancy; diabetic coma; diabetic ketoacidosis; hypersensitivity to tolbutamide, sulfonylureas, or their components; sole therapy for type 1 diabetes mellitus

Interactions

ACE inhibitors, anabolic steroids, androgens, azole antifungals, bromocriptine, chloramphenicol, clofibrate, disopyramide, guanethidine, H2-receptor antagonists, insulin, magnesium salts, MAO inhibitors, methyldopa, octreotide, oxyphenbutazone, phenylbutazone, probenecid, quinidine, salicylates, sulfonamides, tetracycline, theophylline, tricyclic antidepressants, urinary acidifiers: Increased risk of hypoglycemia asparaginase, calcium channel blockers, cholestyramine, clonidine, corticosteroids, danazol, diazoxide, estrogen, glucagon, hydantoins, isoniazid, lithium, morphine, nicotinic acid, oral contraceptives, phenothiazines, rifabutin, rifampin, sympathomimetics, thiazide diuretics, thyroid , urinary alkalizers: Increased risk of hyperglycemia
beta blockers: Possibly hyperglycemia or masking of signs and symptoms of hypoglycemia digoxin: Increased risk of digitalis toxicity pentamidine: Initial hypoglycemia and then hyperglycemia if beta cell damage occurs
alcohol use: Altered blood glucose control (usually hypoglycemia), possibly disulfiramlike reaction

Side Efect

CNS: Dizziness, fatigue, headache, malaise, paresthesia, vertigo
ENDO: Hypoglycemia
GI: Anorexia, cholestasis, heartburn, nausea, vomiting
HEME: Agranulocytosis, aplastic anemia, hemolysis, hemolytic anemia, leukopenia, thrombocytopenia
MS: Muscle weakness
SKIN: Erythema, photosensitivity, pruritus, rash, urticaria

Cautions

If patient takes 20 units or less of insulin daily, expect a possible transfer from insulin to tolbutamide. If patient takes more than 20 units of insulin daily, expect to reduce insulin dosage as tolbutamide therapy starts.

Anticipate that patient receiving tolbutamide may need temporary insulin treatment during periods of physiologic stress, such as fever, surgery, systemic infection, or trauma.

Assess elderly patients for signs of hypoglycemia because they’re more susceptible to drug’s hypoglycemic effect. Anticipate that hypoglycemia may be more difficult to detect.

Assess patient with thyroid disease for altered blood glucose control because thyroid hormone increases GI absorption of glucose.

Expect prescriber to stop tolbutamide 2 weeks before pregnant patient delivers her neonate to minimize the risk of prolonged hypoglycemia in neonate.

PATIENT SAFTY

Advise patient to avoid alcohol while taking tolbutamide.

Teach patient and family members how to monitor blood glucose level and recognize signs of hypoglycemia and hyperglycemia.

Instruct patient to treat mild hypoglycemia with fruit juice or other simple sugars.

Category

Chemical class: Nitrobenzophenone
Therapeutic class: Antidyskinetic

Pregnancy category: C

Indications

As adjunct (with levodopa and carbidopa) to treat Parkinson’s disease
Adults. Initial: 100 mg t.i.d. Maximum: 200 mg t.i.d.

Mechanism of Action

Prolongs plasma half-life of levodopa by inhibiting catechol-O-methyltransferase (COMT), an enzyme responsible for metabolizing catecholamines—including dopa, dopamine, epinephrine, norepinephrine, and their hydroxylated metabolites. COMT inhibition decreases the metabolizing enzyme for levodopa, which yields a more sustained plasma levodopa level, making more available for diffusion into the CNS to be converted to dopamine.

Contraindications

Confusion, hyperpyrexia, or rhabdomyolysis with previous use of tolcapone; hepatic dysfunction; hypersensitivity to tolcapone or its components

Interactions

desipramine: Possibly increased frequency of adverse effects levodopa: Increased levodopa bioavailability, with increased risk of orthostatic hypotension and syncope
MAO inhibitors: Possibly inhibited catecholamine metabolism

Side Efect

CNS: Confusion, dizziness, drowsiness, dyskinesia, fatigue, fever, hallucinations, headache, lethargy, loss of balance
CV: Chest pain, orthostatic hypotension
EENT: Dry mouth
GI: Abdominal pain, acute fulminant liver failure, anorexia, cholestasis, constipation, diarrhea, elevated liver function test results, vomiting
GU: Bright yellow urine, hematuria
MS: Muscle cramps, rhabdomyolysis
RESP: Dyspnea, upper respiratory tract infection
SKIN: Diaphoresis, jaundice
Other: Intense urges to perform certain activities (such as gambling and sex)

Cautions

Ensure that patient has had the risks of tolcapone therapy explained fully to him and has signed the acknowledgement form before starting therapy.

Use cautiously in patient with severe dyskinesia or dystonia because drug is known to cause rhabdomyolysis.

Monitor liver function test results, as ordered, during tolcapone therapy to detect hepatic impairment. Expect to discontinue drug if patient’s liver enzymes exceed twice the upper limit of normal or if patient has any signs or symptoms of liver dysfunction, such as persistent nausea, fatigue, lethargy, anorexia, jaundice, dark urine, pruritus, or right upper quadrant tenderness.

Assess patient for hallucinations, especially in patient over age 75.

Anticipate that drug may precipitate or exaggerate preexisting dyskinesia.

Expect tolcapone to be discontinued if no improvement occurs after 3 weeks of drug therapy.

Assess patient for skin changes regularly because risk of melanoma in higher in patients with Parkinson’s disease. It isn’t clear whether risk results from disease or used to treat it.

PATIENT SAFTY

Inform patient that urine may turn bright yellow during tolcapone therapy.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Urge patient to notify prescriber immediately about darkened urine, decreased appetite, fatigue, jaundice, lethargy, and right-sided abdominal pain.

Caution patient not to stop taking drug abruptly. Explain that prescriber will supervise tapering of drug dosage.

Urge patient to have regular follow-up appointments and laboratory tests.

Urge patient to have regular skin examinations by a dermatologist or other qualified health professional.

Advise patient to notify prescriber about intense urges (as for gambling or sex) because dosage may need to be reduced or drug discontinued.

Category

Chemical class: Pyrroleacetic acid derivative
Therapeutic class: Anti-inflammatory

Pregnancy category: C

(first trimester), Not rated (later trimesters)

Indications

To relieve moderate pain from rheumatoid arthritis and osteoarthritis ,
Adults. Initial: 400 mg t.i.d. Maintenance: 600 to 1,800 mg daily in divided doses t.i.d. or q.i.d. Maximum: 2,000 mg daily for rheumatoid arthritis, 1,600 mg daily for osteoarthritis. To treat juvenile rheumatoid arthritis , Children over age 2. Initial: 20 mg/kg daily in divided doses t.i.d. or q.i.d. Maintenance: 15 to 30 mg/kg daily in divided doses. Maximum: 30 mg/kg daily.

Mechanism of Action

Blocks cyclooxygenase, the enzyme needed to synthesize prostaglandins, which mediate the inflammatory response and cause local vasodilation, swelling, and pain. Prostaglandins also promote pain transmission from the periphery to the spinal cord. By blocking cyclooxygenase and inhibiting prostaglandins, tolmetin reduces inflammatory symptoms and relieves pain.

Contraindications

Angioedema, asthma, bronchospasm, nasal polyps, rhinitis, or urticaria caused by aspirin, iodides, or other NSAIDs

Interactions

ACE inhibitors,
beta blockers: Decreased effectiveness of these , possibly reduced renal function alendronate, corticosteroids, other NSAIDs, salicylates: Possibly adverse GI effects anticoagulants, platelet aggregation inhibitors, thrombolytics: Additive inhibition of platelet aggregation; prolonged bleeding time antineoplastics, antithymocyte globulin, strontium-89 chloride: Increased risk of bleeding cidofovir: Possibly nephrotoxicity cyclosporine: Potentiated cyclosporine nephrotoxicity digoxin: Increased blood digoxin level lithium: Possibly lithium toxicity methotrexate: Increased or prolonged blood methotrexate level
alcohol use: Increased risk of adverse GI effects

Side Efect

CNS: Aseptic meningitis, cerebral hemorrhage, ischemic stroke, depression, dizziness, drowsiness, fatigue, headache, transient ischemic attack, weakness
CV: Chest pain, deep vein thrombosis, edema, hypertension, MI, peripheral edema
EENT: Tinnitus
ENDO: Hypoglycemia
GI: Abdominal pain; constipation; diarrhea; elevated liver function test results; flatulence; gastritis; GI bleeding, perforation, or ulceration; hepatitis; indigestion; jaundice; liver failure; nausea; peptic ulcer disease; vomiting
GU: Acute renal failure, dysuria, elevated BUN level, hematuria, interstitial nephritis, nephrotic syndrome, nephrotoxicity, proteinuria, UTI
HEME: Agranulocytosis, aplastic anemia, hemolytic anemia, leukopenia, pancytopenia, prolonged bleeding time
SKIN: Erythema multiforme, exfoliative dermatitis, maculopapular rash, StevensJohnson syndrome, toxic epidermal necrolysis, urticaria
Other: Anaphylaxis, angioedema, weight gain or loss

Cautions

Give tolmetin with food or milk to reduce adverse GI reactions.

Assess patient for improvement within 7 days and progressive improvement over several successive weeks.

Use tolmetin with extreme caution in patients with a history of ulcer disease or GI bleeding because NSAIDs such as tolmetin increase the risk of GI bleeding and ulceration. Expect to use tolmetin for the shortest time possible in these patients.

Be aware that serious GI tract ulceration, bleeding, and perforation may occur without
WARNING symptoms. Elderly patients are at greater risk. To minimize risk, give drug with food. If GI distress occurs, withhold drug and notify prescriber at once.

Use tolmetin cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.
WARNING Monitor patient closely for thrombotic events, including MI and stroke, because NSAIDs increase the risk.
WARNING If patient has bone marrow suppression or is receiving antineoplastic drug therapy, monitor laboratory results (including WBC count), and watch for evidence of infection because anti-inflammatory and antipyretic actions of tolmetin may mask signs and symptoms, such as fever and pain.

Especially if patient is elderly or taking tolmetin long-term, watch for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.

Monitor liver function test results because, rarely, elevated levels may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.

Monitor BUN and serum creatinine levels in patients with heart failure, impaired renal function, or hepatic dysfunction; those taking diuretics or ACE inhibitors; and elderly patients because drug may cause renal failure.

Monitor CBC for decreased hemoglobin and hematocrit because drug may worsen anemia.

Assess patient’s skin routinely for rash or other signs of hypersensitivity reaction because tolmetin and other NSAIDs may cause serious skin reactions without warning, even in patients with no history of NSAID hypersensitivity. Stop drug at first sign of reaction, and notify prescriber.

Assess invasive sites or wounds for bleeding and bruising from drug’s effects on platelets.

PATIENT SAFTY

Tell patient to take drug with food or milk.

Urge patient to limit sodium intake because drug may cause fluid retention.

Tell patient to avoid alcohol during therapy.

Teach patient how to perform proper oral hygiene, and advise her to have needed dental work done before tolmetin therapy starts because of the increased risk of bleeding.

Explain that tolmetin may increase the risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.

Tell patient that tolmetin also may increase the risk of serious adverse GI reactions; stress the need to seek immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.

Alert patient to the possibility of rare but serious skin reactions. Urge her to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity.

Category

Chemical class: Prodrug of 5-hydroxymethyltolterodine
Therapeutic class: Antispasmodic

Pregnancy category: C

Indications

To treat overactive bladder
Adults. 2 mg b.i.d. Reduced to 1 mg b.i.d. based on patient response and tolerance.
DOSAGE ADJUSTMENT Dosage reduced to 1 mg b.i.d. for patients with significant hepatic or renal dysfunction and for patients who are also receiving cytochrome P-450 3A4 inhibitors, such as clarithromycin, erythromycin, and the antifungals itraconazole, ketoconazole, and miconazole.
Adults. 4 mg daily. Reduced to 2 mg daily based on individual response and tolerance.

Mechanism of Action

Exerts antimuscarinic (atropine-like) and potent direct antispasmodic (papaverinelike) actions on smooth muscle in the bladder, which decreases detrusor muscle contractions. This helps reduce urinary frequency and urgency as well as urge-related incontinence.

Contraindications

Gastric retention, hypersensitivity to tolterodine tartrate or its components, uncontrolled angle-closure glaucoma, urine retention

Interactions

clarithromycin, erythromycin, itraconazole, ketoconazole, miconazole: Possibly increased blood tolterodine level class IA antiarrhythmics (such as quinidine, procainamide) or class III antiarrhythmics (such as amiodarone, sotalol): Possibly increased risk of prolonged QT interval fluoxetine: Possibly decreased tolterodine metabolism

Side Efect

CNS: Confusion, disorientation, dizziness, drowsiness, fatigue, hallucinations, headache, memory impairment, somnolence, worsening of dementia
CV: Chest pain, edema, hypertension, palpitations, QT interval prolongation, tachycardia
EENT: Abnormal vision, blurred vision, dry eyes, dry mouth
GI: Abdominal pain, constipation, diarrhea, flatulence, indigestion, nausea
GU: Dysuria, urine retention, UTI
Other: Anaphylaxis, angioedema, flulike symptoms

Cautions

Use cautiously in patients with decreased GI motility, myasthenia gravis, or narrowangle glaucoma because tolterodine could make these conditions worse.
WARNING Monitor patients with a history of bladder outflow obstruction for decreased urine output or bladder distention because tolterodine poses a risk of urine retention.

Monitor patients with a history of GI obstructive disorders, such as pyloric stenosis, for abdominal distention or bloating because of increased risk of gastric retention.

Be aware that drug’s antimuscarinic effects may produce blurred vision, dizziness, and drowsiness. If these occur, institute fall precautions according to facility policy.

PATIENT SAFTY

Instruct patient taking tolterodine to immediately report to prescriber difficulty urinating or infrequent urination.

Advise patient not to drive or perform activities that require high alertness until drug’s CNS and vision effects are known. Instruct her to notify prescriber if dizziness or blurred vision persists.

Encourage patient to use sugarless candy, gum, or ice to relieve dry mouth. Advise her to notify prescriber or dentist if dry mouth persists or worsens over 2 weeks.

Category

Chemical class: Non-peptide vasopressin receptor antagonist
Therapeutic class: Antihyponatremic

Pregnancy category: C

Indications

To treat significant hypervolemic and euvolemic hyponatremia (serum sodium level less than 125 mEq/L or symptomatic but less-marked hyponatremia that has resisted correction with fluid restriction), including patients with heart failure, cirrhosis, or syndrome of inappropriate antidiuretic hormone (SIADH)
Adults. Initial: 15 mg once daily, increased after at least 24 hours to 30 mg once daily. Maximum: 60 mg once daily.

Mechanism of Action

Raises serum sodium levels by increasing urine output and decreasing urine osmolality. Tolvaptan does this by preventing attachment of vasopressin to vasopressin V2 receptors on cell membranes in the nephron’s collecting duct. Without vasopressin activity, urinary water exrcetion increases.

Contraindications

Acute need to raise serum sodium urgently; anuria; concomitant use of strong CYP3A inhibitors such as clarithromycin, ketoconazole, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin; hypovolemic hypontremia; hypersensitivity to tolvaptan or its components; inability of patient to sense or respond appropriately to thirst

Interactions

ACE inhibitors, angiotensin receptor blockers, potassium sparing diuretics, potassium supplements: Increased risk of hyperkalemia CYP3A inducers such as barbiturates, carbamazepine, phenytoin, rifabutin, rifampin, rifapentin,
St. John’s wort: Decreased serum tolvaptan level and decreased effectiveness CYP3A inhibitors such as aprepitant, clarithromycin, diltiazem, erythromycin, fluconazole, ketoconazole, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, verapamil; P-gp inhibitors such as cyclosporine: Increased serum tolvaptan level and risk of

Side Efect

digoxin: Increased digoxin level grapefruit juice: Increased serum tolvaptan level

Side Efect

CNS: Asthenia, CVA, fever, thirst
CV: Deep vein thrombosis, intracardiac thrombus, ventricular fibrillation
EENT: Dry mouth
ENDO: Diabetic ketoacidosis, hyperglycemia
GI: Anorexia, constipation, gastrointestinal bleeding, ischemic colitis, nausea
GU: Nocturia, polyuria, urethral or vaginal hemorrhage
HEME: Disseminated intravascular coagulation, prolonged prothrombin time
MS: Rhabdomyolysis
RESP: Pulmonary embolism, respiratory failure
Other: Dehydration, hyperkalemia, hyponatremia, hypovolemia

Cautions

Use cautiously in patients with cirrhosis because of increased risk of GI bleeding.
WARNING Give tolvaptan, initially or if reintroduced, in a hospital setting because too-rapid correction of hyponatremia (more than 12 mEq/L in 24 hour) causes osmotic demyelination (affective changes, coma, dysarthria, dysphagia, lethargy, mutism, spastic quadriparesis, seizures, death). If present, notify prescriber immediately and expect to stop tolvaptan and give hypotonic fluids.

Monitor fluid and electrolyte balance regularly, especially when starting tolvaptan and adjusting dosage, as ordered.

Don’t restrict fluids during first 24 hours of therapy because doing so may increase the risk of overly-rapid correct of serum sodium, hypovolemia, and dehydration.

Use of hypertonic saline isn’t recommended during tolvaptan therapy because effects are unknown.

PATIENT SAFTY

Instruct patient to consume fluids according to thirst during first 24 hours of therapy and not to try to limit fluid intake.

When drug is discontinued, tell patient that he’ll need to resume fluid restriction and will need continued monitoring of sodium level and fluid status.

Category

Chemical class: Sulfamate-substituted monosaccharide
Therapeutic class: Anticonvulsant

Pregnancy category: C

Indications

To treat partial-onset or primary generalized tonic-clonic seizures Adults and children age 10 and over. Initial: 25 mg b.i.d. in morning and evening. Increased by 50 mg daily every wk. Maintenance: 200 mg b.i.d. in morning and evening. As adjunct to treat partial seizures and primary generalized tonic-clonic seizures , Adults and adolescents age 17 and over. Initial: 25 to 50 mg daily in divided doses b.i.d. for 1 wk. Increased by 25 to 50 mg daily every wk. Maintenance: 200 to 400 mg daily in divided doses b.i.d. Maximum: 1,600 mg daily. Children ages 2 to 16. Initial: 25 mg or less at bedtime for 1 wk. Increased every 1 to 2 wk by 1 to 3 mg/kg daily in divided doses every 12 hr, as prescribed. Usual: 5 to 9 mg/kg daily in divided doses every 12 hr. As adjunct to treat seizures associated with Lennox-Gastaut syndrome , Children ages 2 to 16. 25 mg at bedtime for 1 wk. Increased every 1 to 2 wk by 1 to 3 mg/kg daily in divided doses every 12 hr, as prescribed. Usual: 5 to 9 mg/kg daily in divided doses every 12 hr. To prevent migraine headache ,
Adults. Initial: 25 mg daily in evening for 1 wk; then 25 mg b.i.d. for 1 wk; then 25 mg in morning and 50 mg in evening for 1 wk. Maintenance: 50 mg b.i.d.
DOSAGE ADJUSTMENT For patients with moderate to severe renal impairment, dosage possibly reduced by 50%.

Mechanism of Action

May block the spread of seizures by reducing the length and frequency of excitatory transmission. Topiramate increases the availability of the inhibitory neurotransmitter gamma-aminobutyric acid by blocking voltage-sensitive sodium channels. This action promotes the movement of chloride ions into neurons.

Contraindications

Hypersensitivity to topiramate or its components

Interactions

antihistamines, barbiturates, benzodiazepines, CNS depressants, opioid analgesics, skeletal muscle relaxants, tricyclic antidepressants: Additive CNS depression carbamazepine: Decreased blood topiramate level carbonic anhydrase inhibitors: Increased risk of renal calculus formation digoxin: Possibly decreased blood digoxin level ethinyl estradiol: Increased risk of breakthrough bleeding oral contraceptives: Increased risk of breakthrough bleeding, decreased contraceptive efficacy phenobarbital: Altered blood phenobarbital level
phenytoin: Decreased blood level of topiramate probenecid: Possibly blocked renal tubular reabsorption of topiramate and decreased blood topiramate level
valproic acid: Decreased blood levels of both , increased risk of hyperammonemia
alcohol use: Additive CNS depression

Side Efect

CNS: Agitation, anxiety, asthenia, ataxia, confusion, decreased concentration, depression, dizziness, encephalopathy, fatigue, fever, hallucinations, headache, hyperthermia, hypoesthesia, insomnia, irritability, memory loss, mood changes, nervousness, paresthesia, psychomotor slowing, psychosis, slurred speech, somnolence, suicidal ideation, syncope, tremor
CV: Cardiac arrest, chest pain, hot flashes, hypertension, hypotension, palpitations, vasodilation
EENT: Blurred vision, diplopia, dry mouth, gingivitis, hearing loss, maculopathy, nystagmus, periorbital pain, pharyngitis, rhinitis, secondary angle-closure glaucoma with acute myopia, sinusitis, taste perversion, tinnitus, tongue edema, vision changes
ENDO: Breast pain, hyperglycemia
GI: Abdominal pain, anorexia, constipation, diarrhea, flatulence, gastroenteritis, gastroesophageal reflux, hepatic failure, hepatitis, indigestion, nausea, pancreatitis, vomiting
GU: Cystitis, decreased libido, dysmenorrhea, dysuria, frequent urination, impotence, menstrual irregularities, renal calculi, renal tubular acidosis, UTI, vaginitis
HEME: Anemia, leukopenia
MS: Arthralgia, back pain, leg cramps or pain, muscle weakness
RESP: Bronchitis, cough, dyspnea, pulmonary embolism, upper respiratory tract infection
SKIN: Acne, alopecia, decreased sweating, erythema multiforme, pemphigus, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Dehydration, hyperammonemia, metabolic acidosis, weight gain or loss

Cautions

Obtain baseline serum bicarbonate level before topiramate therapy and monitor periodically throughout therapy, as ordered.

Use topiramate cautiously in patients with inborn errors of metabolism or impaired hepatic function, or who are taking valproic acid because they may be at higher risk for hyperammonemia with or without encephalopathy while taking topiramate.

Give capsule with water and have patient swallow it whole. If needed, open capsules and empty contents onto a spoonful of soft food. Discard unused portion.

Never store food sprinkled with drug for use at a later time.
WARNING Anticipate an increase in seizures if therapy stops abruptly. Take seizure precautions, as appropriate. Expect drug to be withdrawn gradually if time permits.

If patient reports ocular pain or decreased visual acuity, notify prescriber immediately; topiramate may cause increased intraocular pressure and secondary angleclosure glaucoma. Expect to stop drug immediately.

If patient has a history of renal calculi, assess for signs of recurrence.

PATIENT SAFTY

Instruct patient to swallow topiramate tablets whole.

Urge patient to avoid potentially hazardous activities until drug’s CNS effects are known.

Advise patient to watch for decreased sweating and significantly increased body temperature, especially during hot weather, and to notify prescriber immediately if they occur.

Tell patient to maintain adequate fluid intake to minimize the risk of developing kidney stones.

Advise female patient of possible breakthrough bleeding. If she takes an oral contraceptive, encourage her to use another form of contraception during therapy.

Caution patient not to stop taking topiramate abruptly because seizures may occur. Instead, patient should expect drug to be withdrawn gradually if it needs to be discontinued.

Instruct patient to seek immediate emergency care for blurred vision, other visual disturbances, or periorbital pain.

Urge caregivers to watch patient closely for evidence of suicidal tendencies, especially when topiramate therapy starts or dosage changes, and to report concerns at once to prescriber.

Urge woman who becomes pregnant while taking topiramate to enroll in the North American antiepileptic drug pregnancy registry by calling 1-888-233-2334. Explain that the registry is collecting information about the safety of antiepileptic during pregnancy.

Category

Chemical class: Anilinopyridine sulfonylurea derivative
Therapeutic class: Antihypertensive, diuretic

Pregnancy category: B

Indications

To treat edema in heart failure ,
I.V.INJECTION
Adults. Initial: 10 to 20 mg daily, adjusted by doubling, as prescribed, to achieve desired effect. Maximum: 200 mg daily. To treat edema in chronic renal failure ,
I.V.INJECTION
Adults. Initial: 20 mg daily, adjusted by doubling, as prescribed, to achieve desired effect. Maximum: 200 mg daily. To treat ascites, alone or with amiloride or spironolactone ,
I.V.INJECTION
Adults. Initial: 5 to 10 mg daily. Maximum: 40 mg daily. To manage hypertension
Adults. Initial: 5 mg daily, increased to 10 mg daily after 4 to 6 wk, as prescribed, if response is inadequate. Maximum: 10 mg daily.

Mechanism of Action

Blocks active sodium and chloride reabsorption in the ascending loop of Henle by promoting rapid excretion of water, sodium, and chloride. Torsemide also increases the production of renal prostaglandins, increasing the plasma renin level and renal vasodilation. As a result, blood pressure falls, reducing preload and afterload.

Contraindications

Hypersensitivity to torsemide, sulfonamides, or their components

Interactions

ACE inhibitors, antihypertensives: Additive hypotension amiloride, spironolactone, triamterene: Possibly counteracted torsemide-induced hypokalemia amphotericin B: Increased risk of nephrotoxicity and severe, prolonged hypokalemia or hypomagnesemia cisplatin: Increased risk of significant hypokalemia or hypomagnesemia, possibly permanent ototoxicity cortisone, fluorocortisone, hydrocortisone: Increased risk of sodium retention and hypokalemia digoxin: Increased risk of arrhythmias and digitalis toxicity due to hypokalemia or hypomagnesemia indomethacin: Possibly decreased diuretic and antihypertensive effects of torsemide and increased risk of renal failure lithium: Possibly lithium toxicity metolazone, thiazide diuretics: Increased risk of severe fluid and electrolyte loss neuromuscular blockers: Possibly increased neuromuscular blockade due to hypokalemia probenecid: Possibly decreased diuretic effect of torsemide quinidine and other ototoxic : Increased risk of ototoxicity salicylates: Increased risk of salicylate toxicity
alcohol use: Additive diuresis and, possibly, dehydration

Side Efect

CNS: Dizziness, drowsiness, fatigue, headache, insomnia, lethargy, nervousness, restlessness, weakness
CV: Chest pain, ECG abnormalities, edema, hypotension, tachycardia
EENT: Dry mouth, hearing loss, ototoxicity, pharyngitis, rhinitis, tinnitus
GI: Constipation, diarrhea, indigestion, nausea, thirst, vomiting
GU: Azotemia (prerenal), oliguria, urinary frequency
MS: Muscle spasms, myalgia
RESP: Cough
Other: Hypochloremia, hypokalemia, hypomagnesemia, hyponatremia, hypovolemia

Cautions

Inject I.V. torsemide slowly over 2 minutes. Flush I.V. line with normal saline solution before and afterward.

Don’t exceed 200 mg in a single I.V. dose of torsemide.

Monitor patient’s serum electrolyte levels and fluid intake and output to detect hypovolemia.
WARNING Expect torsemide-induced electrolyte imbalances, such as hypokalemia and hypomagnesemia, to increase the risk of toxicity and fatal arrhythmias in a patient who takes a digitalis glycoside. Hypokalemia also potentiates the neuromuscular blockade effects of nondepolarizing neuromuscular blockers.

PATIENT SAFTY

Advise patient to change position slowly to minimize the effects of orthostatic hypotension.

Instruct patient to notify prescriber at once about drowsiness, dry mouth, hearing changes, lethargy, muscle pain, nausea, restlessness, thirst, vomiting, or weakness.

Advise diabetic patient to monitor her blood glucose level often because drug may raise it.

Category

Chemical class: Cyclohexanol
Therapeutic class: Analgesic

Pregnancy category: C

Indications

To relieve moderate to moderately severe pain Adults and adolescents over age 16. 50 to 100 mg every 4 to 6 hr, p.r.n. Maximum: 400 mg daily.
DOSAGE ADJUSTMENT If patient has hepatic impairment, dosage reduced to 50 mg every 12 hr. If patient is age 75 or over, maximum dosage reduced to 300 mg daily. If creatinine clearance is 30 ml/min/1.73 m2or less, interval increased to every 12 hr and maximum dosage limited to 200 mg daily.
Adults. 100 mg once daily, increased in 100-mg increments once daily every 5 days, as needed. Maximum: 300 mg once daily.

Mechanism of Action

Binds with mu receptors and inhibits the reuptake of norepinephrine and serotonin, which may account for tramadol’s analgesic effect.

Contraindications

Alcohol intoxication; excessive use of central-acting analgesics, hypnotics, opioids, or other psychotropic ; hypersensitivity to tramadol or its components; use within 14 days of MAO inhibitor therapy

Interactions

alpha blockers, CYP2D6 and CYP3A4 inhibitors (amitriptyline, erythromycin, fluoxetine, paroxetine, quinidine), linezolid, lithium, MAO inhibitors, St. John’s wort, selective serotonin and norepinephrine reuptake inhibitors, tricyclic antidepressants, triptans: Increased risk of serotonin syndrome amiodarone, cimetidine, clomipramine, desipramine, fluphenazine, haloperidol, propa-fenone, quinidine, ritonavir, thioridazine: Decreased analgesia, increased adverse effects of tramadol amitriptyline, amphetamines, antipsychotics, bupropion, cyclobenzaprine, dextroamphetamine, erythromycin, fluoxetine, ketoconazole, paroxetine, quinidine, MAO inhibitors, naloxone, tricyclic antidepressants: Increased risk of seizures barbiturates, benzodiazepines, opioid analgesics, sedative-hypnotics, tranquilizers: Additive CNS depression carbamazepine: Increased tramadol metabolism general anesthetics: Increased CNS and respiratory depression phenothiazines,
rifampin: Additive CNS depression, increased risk of seizures
warfarin: Possibly increased INR
alcohol use: Additive CNS depression

Side Efect

CNS: Agitation, anxiety, asthenia, depression, dizziness, emotional lability, euphoria, fatigue, fever, hallucinations, headache, hypertonia, hypoesthesia, insomnia, lethargy, nervousness, paresthesia, restlessness, rigors, seizures, serotonin syndrome, somnolence, suicidal ideation, tremor, vertigo, weakness
CV: Chest pain, orthostatic hypotension, vasodilation
EENT: Blurred vision, dry mouth, nasal or sinus congestion, sore throat, vision changes
ENDO: Hot flashes
GI: Abdominal pain, anorexia, constipation, diarrhea, indigestion, nausea, vomiting
GU: Urinary frequency, urine retention
MS: Arthralgia; back, limb, or neck pain
RESP: Cough, dyspnea
SKIN: Diaphoresis, dermatitis, flushing, pruritus, rash
Other: Flulike illness, physical and psychological dependence

Cautions

Be aware that tramadol shouldn’t be given to patients with a history of anaphylactoid reactions to codeine or other opioids.
WARNING Monitor patient closely for evidence of serotonin syndrome, such as agitation, hallucinations, coma, tachycardia, labile blood pressure, hyperthermia, hyperreflexia, incoordination, nausea, vomiting, or diarrhea. Notify prescriber at once because serotonin syndrome may be life-threatening. Be prepared to discontinue drug and provide supportive care.

Because tramadol may lead to physical and psychological dependence, assess patient for evidence of dependence or abuse. Avoid giving drug to patients with a history of dependence on other opioids.

Avoid giving tramadol to patients with acute abdominal conditions because it may mask evidence and disrupt assessment of the abdomen.

After patient receives first tramadol dose, watch for allergic reactions, including angioedema, bronchospasm, pruritus, Stevens-Johnson syndrome, toxic epidermal necrolysis, and urticaria. Also watch for signs and symptoms of anaphylaxis, such as dyspnea and hypotension.

If patient has respiratory depression, assess respiratory status often, and expect to give a nonopioid analgesic—not tramadol.

If patient develops respiratory depression, expect to give naloxone. Watch for seizures because naloxone may increase this risk. Take seizure precautions.

Assess respiratory status often if patient has increased intracranial pressure or head injury because of possible increased carbon dioxide retention and CSF pressure, either of which may cause respiratory depression. Also, be aware that tramadol may constrict pupils, obscuring evidence of intracranial complications.
WARNING Watch for seizures in patients with epilepsy, a history of seizures, or an increased risk of seizures, such as those with head injury, metabolic disorders, alcohol or drug withdrawal, or CNS infection.

Expect to taper tramadol rather than stopping it abruptly to avoid such acute withdrawal symptoms as anxiety, diarrhea, insomnia, nausea, pain, panic attacks, paresthesias, piloerection, rigors, sweating, tremor, and upper respiratory symptoms.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

PATIENT SAFTY

Urge patient to follow prescribed dose limits and dosing intervals to prevent respiratory depression and seizures.

Instruct patient prescribed extendedrelease form to swallow tablet whole and not to chew, crush, or split tablet.

Caution patient not to stop tramadol abruptly.

Instruct patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to avoid alcohol while taking tramadol.

Urge patient to notify prescriber about known, suspected, or intended pregnancy.

Urge caregivers to watch patient closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes and to report concerns at once to prescriber.

Tell patient to notify prescriber immediately if he develops any sudden onset, unusual, persistent, or severe adverse reactions.

Category

Chemical class: ACE inhibitor (nonsulfhydryl-containing)
Therapeutic class: Antihypertensive, vasodilator

Pregnancy category: C

(first trimester), D (later trimesters)

Indications

To manage hypertension
Adults. Initial: 1 mg daily, increased every wk based on clinical response. Dosage may be given in two daily doses if antihypertensive effect diminishes before 24 hr. Usual: 2 to 4 mg daily. Maximum: 8 mg daily.
DOSAGE ADJUSTMENT Initial dosage increased to 2 mg daily for blacks with hypertension. Initial dosage reduced to 0.5 mg for patients also receiving a diuretic, those with a creatinine clearance of less than or equal to 30 ml/min/1.73 m2, and those with cirrhosis. To treat heart failure after MI
Adults. Initial: 1 mg daily. Usual: 4 mg or more daily. Maximum: 8 mg daily.

Mechanism of Action

Reduces blood pressure by inhibiting the conversion of angiotensin I to angiotensin II. Angiotensin II is a potent vasoconstrictor that stimulates the renal cortex to secrete aldosterone. Decreased release of aldosterone reduces sodium and water retention and increases their excretion, thereby reducing blood pressure. Trandolapril may also inhibit renal and vascular production of angiotensin II.

Contraindications

History of angioedema related to previous treatment with ACE inhibitor, hypersensitivity to trandolapril or its components

Interactions

allopurinol, bone marrow depressants (such as methotrexate), corticosteroids (systemic), cytostatic , procainamide: Increased risk of potentially fatal neutropenia or agranulocytosis antacids: Decreased blood trandolapril level cyclosporine, potassium-containing , potassium-sparing diuretics, potassium supplements: Increased risk of hyperkalemia diuretics, other antihypertensives: Increased hypotensive effects lithium: Increased blood lithium level and risk of lithium toxicity NSAIDs, sympathomimetics: Possibly reduced antihypertensive effects sodium aurothiomalate: Increased risk of nitroid reactions such as facial flushing, nausea, vomiting, and hypotension high-potassium diet, low-sodium milk, potassium-containing salt substitutes: Increased risk of hyperkalemia
alcohol use: Possibly increased hypotensive effect

Side Efect

CNS: Dizziness, fatigue, fever, headache
CV: Hypotension, orthostatic hypotension
EENT: Loss of taste
GI: Diarrhea, nausea
GU: Decreased libido, impotence
MS: Myalgia
RESP: Cough, dyspnea, upper respiratory tract infection
SKIN: Pruritus, rash
Other: Angioedema

Cautions

WARNING Closely monitor blood pressure during first 2 weeks of therapy and whenever dosage is adjusted, especially in patients with heart failure, hyponatremia, or severe volume or sodium loss. If excessive hypotension occurs, notify prescriber immediately, place patient in supine position, and infuse I.V. normal saline solution, as prescribed.
WARNING Be alert for signs and symptoms of angioedema. If swelling of tongue, glottis, or larynx causes airway obstruction, notify prescriber and be prepared to discontinue drug and administer emergency measures, including subcutaneous epinephrine 1:1,000 (0.3 to 0.5 ml).

Continue to monitor patient’s blood pressure to assess drug’s long-term effectiveness.

PATIENT SAFTY

Instruct patient to notify prescriber immediately and stop taking trandolapril if she experiences swelling of face, eyes, lips, or tongue or has difficulty breathing.

Explain that drug may cause dizziness and light-headedness, especially during first few days of therapy. Advise patient to avoid driving and other potentially hazardous activities until drug’s CNS effects are known and to notify prescriber immediately if she faints.

Inform female patient of childbearing age about risks of taking trandolapril during pregnancy, especially during second and third trimesters. Urge her to use effective contraceptive method and to notify prescriber immediately if she becomes or thinks she might be pregnant.

Advise patient planning to undergo surgery or anesthesia to inform specialist that she’s taking trandolapril.

Instruct patient to consult prescriber before using potassium supplements or salt substitutes containing potassium.

Inform patient about possible loss of taste, which may result in weight loss. Reassure her that loss of taste is usually reversed after 2 to 3 months.

Category

Chemical class: Synthetic lysine amino acid derivative
Therapeutic class: Antifibrinolytic

Pregnancy category: B

Indications

To treat cyclic heavy menstrual bleeding
Adults. 1,300 mg three times daily for a maximum of 5 days during monthly menstruation
DOSAGE ADJUSTMENT For patient with a serum creatinine level above 1.4 mg/dl but equal to or less than 2.8 mg/dl, 1,300 mg two times a day for a maximum of 5 days during menstruation; for patient with a serum creatinine level above 2.8 mg/dl but equal to or less than 5.7 mg/dl, 1,300 mg once daily for a maximum of 5 days during menstruation; for patient with a serum creatinine level above 5.7 mg/dl, 650 mg once daily for a maximum of 5 days during menstruation.

Mechanism of Action

Displaces plasminogen from surface of fibrin by binding to high-affinity lysine site of plasminogen. This diminishes dissolution of hemostatic fibrin, which decreases bleeding.

Contraindications

Active thromboembolic disease; history or intrinsic risk of thrombosis or thromboembolism, including retinal vein or artery occlusion; hypersensitivity to tranexamic acid or its components

Interactions

anti-inhibitor coagulant concentrates, factor IX complex concentrates, hormonal contraceptives: Increased thrombotic risk tissue plasminogen activators: Possibly decreased effectiveness of both tranexamic acid and the tissue plasminogen activator tretinoin (oral): Possibly exacerbation of the pro-coagulant effect of tretinoin

Side Efect

CNS: Cerebral thrombosis, dizziness, fatigue, headache, migraine
CV: Deep vein thrombosis
EENT: Central retinal artery and vein obstruction, feeling of throat tightness, impaired color vision, ligneous conjunctivitis, nasal and sinus congestion, sinusitis, visual abnormalities
GI: Abdominal pain, diarrhea, nausea, vomiting
GU: Acute renal cortical necrosis
HEME: Anemia
MS: Arthralgia, back pain, muscle cramps and spasms, myalgia
RESP: Dyspnea, pulmonary embolism, respiratory congestion,
SKIN: Allergic skin reactions, facial flushing
Other: Anaphylaxis, multiple allergies including seasonal

Cautions

Tranexamic acid therapy isn’t recommended for women who use hormonal contraceptives or who take factor IX complex concentrates or anti-inhibitor coagulant concentrates because of the increased risk of thromboembolism.

Use tranexamic acid cautiously in patients with acute promyelocytic leukemia taking oral tretinoin for remission induction because of possible exacerbation of the pro-coagulant effect of tretinoin.

Cerebral edema and cerebral infarction may occur in women taking tranexamic acid if a subarachnoid hemorrhage occurs.
WARNING Monitor patient closely for allergic reactions to tranexamic acid such as dyspnea, a feeling of throat tightness, and facial flushing that may require emergency medical treatment.

PATIENT SAFTY

Instruct patient to swallow tranexamic acid tablets whole, without chewing or breaking them. Therapy shouldn’t exceed 5 days during menstruation.

Tell patient to seek emergency care immediately if she has any signs of allergic reaction, especially dyspnea, a feeling of throat tightness, and facial flushing, and to stop taking drug.

Advise patient to report any changes in vision or ocular discomfort.

Category

Chemical class: Nonhydrazine derivative
Therapeutic class: Antidepressant

Pregnancy category: Not rated

Indications

To treat major depressive episodes without melancholia Adults and adolescents over age 16. 30 mg/ day in divided doses. After first 2 wk, increased by 10 mg every 1 to 2 wk, as prescribed. Maintenance: 10 to 40 mg daily. Maximum: 60 mg daily.
DOSAGE ADJUSTMENT For elderly patients, initial dosage possibly reduced to 2.5 to 5 mg daily and increased by 2.5 to 5 mg every 3 to 4 days, as prescribed; maximum dosage 45 mg daily. Alternative therapies should be carefully considered for patients over age 60.

Mechanism of Action

Reversibly binds to MAO, reducing its activity and resulting in increased levels of neurotransmitters, including dopamine, epinephrine, and norepinephrine. This regulation of CNS neurotransmitters helps ease depression.

Contraindications

Cardiovascular disease; cerebrovascular disease; heart failure; hepatic disease; history of headaches; hypersensitivity to tranylcypromine or its components; hypertension; pheochromocytoma; severe renal impairment; use of anesthetics, antihypertensives, bupropion, buspirone, carbamazepine, CNS depressants, cyclobenzaprine, dextromethorphan, meperidine, other MAO inhibitors, selective serotoninreuptake inhibitors, sympathomimetics, or tricyclic antidepressants

Interactions

amoxapine, bupropion, maprotiline, selective norepinephrine reuptake inhibitors, selective serotonin reuptake inhibitors, trazodone, tricyclic antidepressants: Increased risk of severe hypertensive crisis, increased anticholinergic effects anticonvulsants: Additive CNS depression antihistamines: Possibly prolonged anticholinergic and CNS depressant effects antipsychotics: Additive anticholinergic, hypotensive, and sedative effects
beta blockers: Possibly worsened bradycardia bromocriptine: Increased blood prolactin level and interference with bromocriptine effects buspirone: Increased blood pressure dextroamphetamine, isometheptene, local anesthetics, naphazoline, oxymetazoline, psychostimulants, sympathomimetics, tetrahydrozoline, xylometazoline: Increased risk of severe hypertensive reaction dextromethorphan, tryptophan: Increased risk of serotonin syndrome diuretics: Additive hypotensive effects doxapram: Increased vasopressor effects furazolidone, procarbazine, selegiline: Increased risk of severe hyperpyretic or hypertensive crisis, seizures, or death guanadrel, guanethidine: Increased risk of moderate to severe hypertension insulin, oral antidiabetic : Possibly prolonged hypoglycemic response levodopa: Increased vasopressor effects, hypertension, adverse cardiovascular effects meperidine: Increased risk of coma, diaphoresis, excitation, hypertension, rigidity, severe respiratory depression, shock, and, possibly, death methyldopa: Increased risk of hallucinations metrizamide,
tramadol: Increased risk of seizures succinylcholine: Possibly prolonged succinylcholine effects aged cheese; avocadoes; bananas; fava or broad beans; cured sausage (bologna, pepperoni, salami, and summer sausage) or other meat; overripe fruit; pickled fish, meats, or poultry; protein extract; smoked fish, meats, or poultry; soy sauce; yeast extract; and other high in pressor amines, such as tyramine: Increased risk of sudden, severe hypertension caffeine-containing beverages and : Increased risk of severe hypertensive crisis and dangerous arrhythmias alcohol-containing products that also may contain tyramine, such as beer (including reduced-alcohol and alcohol-free beer), wine (red and white), sherry, hard liquor, liqueurs: Increased risk of hypertensive crisis

Side Efect

CNS: Anxiety, chills, dizziness, drowsiness, fever, headache, insomnia, intracranial hemorrhage, paresthesia, restlessness, suicidal ideation, tremor, weakness
CV: Bradycardia, chest pain, edema, hypertensive crisis, orthostatic hypotension, palpitations, tachycardia
EENT: Blurred vision, dry mouth, mydriasis, photophobia, tinnitus
GI: Abdominal pain, anorexia, constipation, diarrhea, nausea, vomiting
GU: Ejaculation disorders, impotence, urine retention
HEME: Agranulocytosis, anemia, leukopenia, thrombocytopenia
MS: Muscle spasms,myoclonus,neck stiffness
SKIN: Clammy skin, diaphoresis

Cautions

Monitor patient’s blood pressure during tranylcypromine therapy to detect hypertensive crisis and to decrease the risk of orthostatic hypotension.
WARNING Notify prescriber immediately if patient has evidence of hypertensive crisis, such as chest pain, headache, neck stiffness, and palpitations. Expect to stop drug right away.

Anticipate that therapeutic response may not occur for up to 4 weeks.

Expect drug to aggravate symptoms of Parkinson’s disease, including muscle spasms, myoclonic movement, and tremor.

Keep dietary restrictions in place for at least 2 weeks after stopping tranylcypromine because of the slow recovery from drug’s enzyme-inhibiting effects.

Expect to stop tranylcypromine 10 days before elective surgery, as prescribed, to avoid hypotension.

Be aware that abrupt cessation of drug can precipitate original symptoms.

Check diabetic patient’s blood glucose level often to detect loss of control.

Anticipate that coadministration with a selective serotonin reuptake inhibitor may cause confusion, seizures, severe hypertension, and other, less severe symptoms.

Monitor severely depressed patients, including children and teens, for suicidal tendencies. Take safety measures, and notify prescriber immediately.

Assess patient for sudden insomnia. If it develops, notify prescriber and be prepared to administer drug early in the day.

PATIENT SAFTY

Instruct patient to avoid that contain cheese and that are high in tyramine, such as anchovies, avocadoes, bananas, beer, canned figs, caviar, Chianti wine, chocolate, dried fruit, fava beans, liqueurs, meat tenderizers, overripe fruit, pickled herring, raspberries, sauerkraut, sherry, sour cream, soy sauce, yeast extract, and yogurt while taking tranylcypromine.

Urge patient to continue dietary restrictions for at least 2 weeks after tranylcypromine therapy stops.

Advise patient to notify prescriber at once about chest pain, dizziness, headache, nausea, neck stiffness, palpitations, rapid heart rate, sweating, and vomiting.

Urge patient to avoid alcohol and excessive caffeine intake during therapy.

Urge patient to change position slowly to minimize orthostatic hypotension.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Caution patient not to take any other prescribed or OTC without consulting prescriber.

Caution patient not to stop drug abruptly to avoid recurrence of original symptoms.

Instruct female patient to use effective contraception during tranylcypromine therapy to prevent fetal abnormalities. Urge her to notify prescriber immediately about known or suspected pregnancy.
WARNING Urge parents to watch their child or adolescent closely for abnormal thinking or behavior or increased aggression or hostility. Stress importance of notifying prescriber about unusual changes.

Category

Chemical class: Triazolopyridine derivative
Therapeutic class: Antidepressant, anxiolytic

Pregnancy category: C

Indications

To treat major depression, with or without generalized anxiety
Adults. Initial: 150 mg daily in divided doses, increased by 50 mg daily every 3 to 4 days, p.r.n., as prescribed. Maximum: 400 mg daily for outpatients, 600 mg daily for inpatients. Children ages 6 to 18. Initial: 1.5 to 2 mg/ kg daily in divided doses, increased every 3 to 4 days, p.r.n., as prescribed. Maximum: 6 mg/kg daily in divided doses.

Mechanism of Action

Blocks serotonin reuptake along the presynaptic neuronal membrane, causing an antidepressant effect. Trazodone exerts an alpha-adrenergic blocking action and produces modest histamine blockade, causing a sedative effect. It also inhibits the vasopressor response to norepinephrine, which reduces blood pressure.

Contraindications

Hypersensitivity to trazodone or its components, recovery from acute MI

Interactions

anticonvulsants: Decreased seizure threshold antihypertensives: Increased risk of excessive hypotension anxiolytics, brompheniramine, carbinoxamine, chlorpheniramine, clemastine, dimenhydrinate, diphenhydramine, doxylamine, general anesthetics, methdilazine, opioid analgesics, phenothiazines, sedative-hypnotics, skeletal muscle relaxants: Increased CNS depression, increased risk of respiratory depression and hypotension barbiturates: Decreased seizure threshold and barbiturate effects, increased drowsiness buspirone, selective serotonin-reuptake inhibitors, tricyclic antidepressants: Possibly excessive serotonergic stimulation carbamazepine: Decreased trazodone level
clonidine: Interference with clonidine’s antihypertensive effect digoxin: Possibly increased blood digoxin level and risk of digitalis toxicity erythromycin, indinavir, itraconazole, ketoconazole, nefazodone, protease inhibitors, ritonavir: Possibly increased blood trazodone level with increased risk of adverse effects
MAO inhibitors: Increased serotonin effects
warfarin: Decreased anticoagulation response
alcohol use: Increased CNS depression, risk of respiratory depression and hypotension

Side Efect

CNS: Dizziness, drowsiness, fatigue, headache, light-headedness, nervousness, suicidal ideation, syncope, tremor
CV: Arrhythmias, hypotension, orthostatic hypotension, palpitations
EENT: Blurred vision, dry mouth
GI: Constipation, indigestion, nausea, vomiting
GU: Anorgasmia, ejaculation disorders, increased libido, priapism
SKIN: Pruritus, rash

Cautions

Give trazodone shortly after the patient has a meal or light snack to reduce nausea.

Give larger portion of daily dose at bedtime if drowsiness occurs.

Because trazadone’s

Mechanism of Action

is similar to that of selective serotonin reuptake inhibitors, expect high doses (6 to 8 mg/kg) to increase blood serotonin level and low doses (0.05 to 1 mg/kg) to decrease blood serotonin level.

Expect most patients who respond to trazodone to do so by the end of the second week of therapy.

Closely monitor depressed patients, including children and teens, for suicidal thoughts and tendencies. Notify prescriber if they occur, and take suicide precautions according to facility policy.

Be aware that adverse CNS reactions usually improve after patient completes a few weeks of therapy.
WARNING Be aware that trazodone therapy may increase the risk of priapism.

PATIENT SAFTY

Urge patient to avoid taking trazodone on an empty stomach because doing so may increase the risk of dizziness or lightheadedness.

Caution patient to avoid potentially hazardous activities during therapy.

Advise patient not to fast during trazodone therapy because of possible adverse CNS reactions.

Instruct male patient to notify prescriber immediately about priapism.
WARNING Urge parents to watch their child or adolescent closely for abnormal thinking or behavior or increased aggression or hostility. Stress importance of notifying prescriber about unusual changes.

Category

Chemical class: Prostaglandin, tricyclic benzidene analog
Therapeutic class: Vasodilator

Pregnancy category: B

Indications

To treat pulmonary artery hypertension in patients who have New York Heart Association Class II to IV symptoms in order to diminish exercise-induced symptoms
IV:, SUBCUTANEOUS INFUSION (REMODULIN)
Adults. Initial: 1.25 nanograms/kg/min. Maintenance: Infusion rate increased in increments of no more than 1.25 nanograms/kg/min each wk for first 4 wk, and in increments of no more than 2.5 nanograms/kg/ min each wk thereafter, as needed. Maximum: 40 nanograms/kg/min.
DOSAGE ADJUSTMENT If initial dosage isn’t tolerated or if patient has mild to moderate hepatic insufficiency, decrease to 0.625 nanogram/kg/min (using ideal body weight). ORAL INHALATION(TYVASO)
Adults. Initial: 18 mcg (3 breaths) four times daily, evenly spaced at 4 hr apart while awake. Increased in 1 to 2 wk to 36 mcg (6 breaths) four times daily, evenly spaced at 4 hr apart while awake. Then increased in another 1 to 2 wk to 54 mcg (9 breaths) four times daily evenly spaced 4 hr apart while awake, as tolerated. Maintenance: 54 mcg (9 breaths) four times daily, evenly spaced at 4 hr apart while awake. Maximum: 54 mcg (9 breaths) four times daily, evenly spaced at 4 hr apart while awake.
DOSAGE ADJUSTMENT For patient unable to tolerate initial dose, dosage decreased to 6 mcg (1 breath) or 12 mcg (2 breaths) four times daily, evenly spaced at 4 hours apart while awake, and then increased to 18 mcg (3 breaths) four times daily, evenly spaced at 4 hr apart while awake when tolerated. Then increased gradually every 1 to 2 wk to achieve target range of 54 mcg or highest tolerated dose.

Mechanism of Action

Acts directly on pulmonary and systemic arterial vascular beds to produce vasodilation.Vasodilatory effects reduce right and left ventricular afterload and increase cardiac output and stroke volume. These effects improve symptoms of pulmonary hypertension, such as dyspnea, and enable patients with pulmonary hypertension to walk farther with less discomfort.

Contraindications

Hypersensitivity to treprostinil, its components, or structurally related compounds

Interactions

anticoagulants: Increased risk of bleeding antihypertensives, diuretics, other vasodilators: Increased risk of hypotension cytochrome P-450 inhibitors such as gemfibrozil: Increased plasma trepostinil level and increased risk of adverse effects cytochrome P-450 inducers such as
rifampin: Decreased plasma trepostinil level and decreased effectiveness

Side Efect

CNS: Anxiety, dizziness, fatigue, headache, restlessness
CV: Chest pain, edema, hypotension, right ventricular heart failure, vasodilatation
EENT: Epistaxis, jaw pain, pharyngolaryngeal pain (inhalation form), throat irritation (inhalation form)
GI: Diarrhea, nausea, vomiting
HEME: Bleeding, thrombocytopenia
RESP: Cough (inhalation form), dyspnea, hemoptysis (inhalation form), wheezing (inhalation form)
MS: Bone or jaw pain
SKIN: Cellulitis, pallor, pruritus, rash
Other: Infusion site pain or reaction (erythema, hematoma, induration, pain, paresthesia, rash, swelling, thrombophlebitis)

Cautions

Use treprostinil cautiously in patients with hepatic or renal impairment becuase of increased risk of adverse effects.

Assess patient’s ability to care for an I.V. or subcutaneous catheter and to use an infusion pump. Discuss findings with prescriber before starting treprostinil therapy.

Be aware that drug shouldn’t be diluted when given subcutaneously.

When drug will be given I.V., dilute with sterile water for injection or normal saline solution according to instructions provided. Watch for blood-borne infections and sepsis in patients receiving drug through an indwelling central venous catheter, which increases the risk.

Calculate infusion rate using the formula provided in the package insert, or refer to charts in package insert to find infusion delivery rate for prescribed dosage and administration route.
WARNING Don’t abruptly stop treprostinil infusion or make sudden large reductions in dose because symptoms of pulmonary hypertension may worsen.

When giving drug by inhalation, use only the Tyvaso inhalation system.

Assess patient often for drug effectiveness and for

Side Efect

. Know that the goal of
DOSAGE ADJUSTMENTs is to find a dose that will improve symptoms of pulmonary hypertension, such as dyspnea and fatigue, while minimizing adverse effects, such as headache, nausea, vomiting, restlessness, anxiety, and infusion site pain or reaction.

Monitor patient’s platelet count and assess patient often for bleeding because drug may increase risk of bleeding episodes.

Be aware that patient must be discharged with a backup infusion pump. It should be adjustable to about 0.002 ml/hr and have alarms that indicate occlusion/no delivery, low battery, programming error, and motor malfunction. Also, the pump should have a delivery accuracy of 66% or better, be positive-pressure driven, and have a reservoir made of polyvinyl chloride, polypropylene, or glass. Make sure patient has additional I.V. or subcutaneous infusion sets to prevent potential interruptions in drug delivery. Likewise, patient prescribed drug via inhalation must be discharged with a backup inhalation system.

PATIENT SAFTY

Explain to patient that treprostinil is infused continuously through an I.V. or subcutaneous catheter via an infusion pump.

Teach patient to operate and maintain the I.V. or subcutaneous infusion pump and to recognize the drug’s adverse effects.

To reduce the risk of infection, caution patient to always use aseptic technique when preparing and giving drug.

Tell patient that a vial of drug shouldn’t be used beyond 14 days after opening (for I.V. or subcutaneous use) and that once the drug is placed in the pump’s reservoir, it shouldn’t be used after 72 hours.

Instruct patient to store treprostinil vials at room temperature (about 25° C [77° F]).

Teach patient prescribed inhalation form of drug how to use the inhalation system and how to clean it after last treatment of the day. Advise patient always to have a backup device in case of malfunction. Make sure patient understands that no other drug should be mixed with treprostinil in medication cup before administration. Explain that each ampule contains enough drug for all 4 treatments for a day. Tell him to twist off the top of ampule before first treatment of the day and squeeze entire contents into medication cup. Dose is controlled by how many breaths he takes. In between treatments, inhalation device should be capped and stored in an upright position.

Caution patient to avoid skin or eye contact with treprostinil solution. If it occurs, instruct patient to flush area immediately with water.

Inform patient that drug will be needed for prolonged periods, possibly years. Stress the importance of not stopping drug abruptly or making sudden large reductions in dosage without consulting prescriber because symptoms could worsen.

Make sure patient understands that treprostinil use doesn’t preclude the subsequent use of an alternative I.V. prostacyclin therapy such as epoprostenol.

Make sure patient has emergency contact information for problems or questions about giving treprostinil at home.

Category

Chemical class: Synthetic glucocorticoid
Therapeutic class: Anti-inflammatory, immunosuppressant

Pregnancy category: C

(nasal and oral inhalation), Not rated (oral and parenteral)

Indications

To prevent bronchospasm or provide long-term corticosteroid treatment to control asthma ORAL INHALATION(TRIAMCINOLONE ACETONIDE) Adults and children age 12 and over. Initial: 2 metered sprays (200 mcg) t.i.d. or q.i.d. Maintenance: Individualized dosage given b.i.d. Maximum: 16 metered sprays daily in divided doses. Children ages 6 to 11. 2 to 4 metered sprays (200 to 400 mcg) b.i.d. to q.i.d. Maximum: 12 metered sprays daily. To treat acute rheumatic carditis, berylliosis, and Hodgkin’s disease; as adjunct to treat fulminating or disseminated pulmonary tuberculosis (with appropriate antituberculosis therapy) SYRUP(TRIAMCINOLONE DIACETATE), (TRIAMCINOLONE) Adults and children age 12 and over. Initial: 4 to 48 mg daily as a single dose or in divided doses. Some patients may require an initial dose of 60 mg. Children under age 12. 0.42 to 1.7 mg/kg daily as a single dose or in divided doses.
I.M.INJECTION(TRIAMCINOLONE ACETONIDE) Adults and children age 12 and over. 40 to 80 mg every 4 wk, as needed. Children ages 6 to 11. 40 mg every 4 wk, as needed,or 30 to 200 mcg/kg every 1 to 7 days.
I.M.INJECTION(TRIAMCINOLONE DIACETATE) Adults and children age 12 and over.40 mg every wk, or 4 to 7 times the daily P.O. dose as a single injection every 4 days to every 4 wk. Children ages 6 to 11. 40 mg/wk. To relieve inflammation caused by acute gouty arthritis, acute nonspecific tenosynovitis, acute or subacute bursitis, epicondylitis, osteoarthritis, posttraumatic osteoarthritis, rheumatoid arthritis, and synovitis SYRUP(TRIAMCINOLONE DIACETATE) Adults and children age 12 and over. 4 to 48 mg daily as a single dose or in divided doses, adjusted, as prescribed, to lowest effective dose based on clinical response. (TRIAMCINOLONE) Adults and children age 12 and over.8 to 16 mg daily in divided doses t.i.d. or q.i.d., adjusted, as prescribed, to lowest effective dose based on clinical response. SYRUP(TRIAMCINOLONE DIACETATE), (TRIAMCINOLONE) Children ages 6 to 11. 0.42 to 1.7 mg/kg daily as a single dose or in divided doses, adjusted based on clinical response.
I.M.INJECTION(TRIAMCINOLONE ACETONIDE) Adults and children age 12 and over.40 to 80 mg every 4 wk. Children ages 6 to 11. 40 mg every 4 wk.
I.M.INJECTION(TRIAMCINOLONE DIACETATE) Adults and children age 6 and over. 40 mg every wk as single injection, repeated every 4 wk if needed. INTRA-ARTICULAR OR INTRABURSAL INJECTION (TRIAMCINOLONE ACETONIDE) Adults and children age 6 and over.2.5 to 15 mg, as needed. INTRA-ARTICULAR OR INTRASYNOVIAL INJECTION (TRIAMCINOLONE DIACETATE)
Adults. 5 to 40 mg, repeated as prescribed every 1 to 8 wk, as needed. INTRA-ARTICULAR INJECTION(TRIAMCINOLONE HEXACETONIDE)
Adults. 2 to 20 mg, repeated as prescribed every 3 to 4 wk, as needed. To treat primary (Addison’s disease) or secondary adrenocortical insufficiency SYRUP(TRIAMCINOLONE DIACETATE) Adults and children age 12 and over.4 to 12 mg daily as a single dose or in divided doses. SYRUP(TRIAMCINOLONE DIACETATE), (TRIAMCINOLONE) Children ages 6 to 11. 0.12 mg (base)/kg daily as a single dose or in divided doses. To treat inflammatory dermatoses (TRIAMCINOLONE) Adults and children age 12 and over. 8 to 16 mg daily. Usual: 1 to 2 mg daily. To treat disseminated lupus erythematosus (TRIAMCINOLONE) Adults and children age 12 and over. 20 to 30 mg daily. Usual: 3 to 30 mg daily. To treat nephrotic syndrome (TRIAMCINOLONE) Adults and children age 12 and over. 16 to 20 mg daily. To relieve symptoms of perennial and seasonal allergic rhinitis (TRIAMCINOLONE) Adults and children age 12 and over.8 to 12 mg daily. Usual: 2 to 6 mg daily. Children ages 6 to 11. 0.42 to 1.7 mg/kg daily as a single dose or in divided doses. NASAL INHALATION(NASACORT) Adults and children age 12 and over. Initial: 220 mcg daily in 2 sprays (55 mcg each)/nostril. Maintenance: 110 mcg daily in 1 spray (55 mcg)/nostril. Maximum: 440 mcg (8 sprays daily). NASAL INHALATION(NASACORT AQ) Adults and children age 12 and over. Initial: 110 mcg daily in 2 sprays (55 mcg each)/nostril. Maintenance: 55 mcg daily in 1 spray/ nostril. Maximum: 220 mcg or 4 sprays daily. Children ages 6 to 11. 110 mcg daily in 1 spray (55 mcg each)/nostril. Maximum: 220 mcg or 4 sprays daily. Children ages 2 to 5. 110 mcg daily in 1 spray (55 mcg)/nostril. Maximum: 100 mcg or 2 sprays daily. NASAL INHALATION(NASACORT HFA) Adults and children age 12 and over. Initial: 220 mcg daily in 2 sprays (55 mcg each)/nostril. May be increased to 440 mcg daily in 4 sprays/nostril, as needed. Children ages 6 to 11. 220 mcg daily in 2 sprays (55 mcg each)/nostril. NASAL INHALATION(ALLERNAZE) Adults and children age 12 and over. Initial: 200 mcg daily in 2 sprays (50 mcg each)/nostril. Maximum: 400 mcg daily in 4 sprays (50 mcg each)/nostril or divided into 2 daily doses. To treat chronic idiopathic thrombocytopenic purpura Adults and children age 12 and over. 0.8 mg/kg daily.

Mechanism of Action

Inhibits the release of prostaglandins and leukotrienes, thus reducing immediate and late-phase allergic responses in chronic asthma. Triamcinolone also:

decreases peribronchial edema and mucus secretion by inhibiting the binding of allergens to immunoglobulin E antibodies on the surface of mast cells, thereby inactivating the release of chemotactic substances

decreases inflammation by interfering with leukocyte adhesion to capillary walls

inhibits the release of leukocytic acid hydrolases, preventing macrophage accumulation at the infection site

inhibits histamine and kinin release, preventing the formation of scar tissue.

Incompatibilities

Don’t mix triamcinolone hexacetonide with parenteral local anesthetics because precipitation can occur.

Contraindications

Acute status asthmaticus (inhalation form), hypersensitivity to triamcinolone or its components, live-virus vaccine therapy, systemic fungal infection

Interactions

amphotericin B, ethacrynic acid, furosemide, thiazide diuretics: Increased potassiumwasting effect, severe hypokalemia aspirin: Increased blood salicylate level, increased risk of salicylate toxicity barbiturates, carbamazepine, phenytoin,
rifampin: Increased triamcinolone metabolism
cholinesterase inhibitors: Increased risk of severe muscle weakness in patients with myasthenia gravis digitalis glycosides: Increased risk of arrhythmias and digitalis toxicity estrogens: Increased triamcinolone effects insulin, oral antidiabetic : Increased blood glucose level isoproterenol: Increased risk of cardiotoxicity live-virus vaccines: Decreased antibody response, increased risk of neurologic complications neuromuscular blockers: Increased risk of hypokalemia and enhanced neuromuscular blockade
NSAIDs: Increased risk of adverse GI effects toxoids: Decreased resistance to toxoids

Side Efect

CNS: Dizziness, emotional lability, exacerbated psychosis, fatigue, headache, insomnia, restlessness, seizures, vertigo
CV: Edema, heart failure, hypertension
EENT: Altered sense of smell or taste, cataracts, dry mouth, epistaxis (nasal form), glaucoma, hoarseness, nasal congestion, nasal irritation (inhalation form), nasal septal perforation (nasal form), oropharyngeal candidiasis, pharyngitis, posterior subcapsular cataracts, rhinorrhea, secondary ocular infection, sinusitis, sneezing
ENDO: Cushing’s syndrome, diabetes mellitus, growth retardation (children)
GI: Abdominal pain, constipation, diarrhea, dyspepsia, esophageal ulceration, gastritis, nausea, vomiting
GU: Cystitis, renal disease, UTI, vaginitis
MS: Bone mineral density loss, bursitis, muscle wasting or weakness, myalgia, osteoporosis, tenosynovitis
RESP: Asthma, bronchitis, bronchospasm (inhalation form), chest congestion, dyspnea, increased cough form), photosensitivity, pruritus, rash, striae, urticaria
Other: Anaphylaxis; angioedema; facial edema; flu syndrome; herpes infection; impaired wound healing; injection site atrophy, induration, pain, soreness, and sterile abscess; weight gain

Cautions

Be aware that high doses of corticosteroids such as trimcinolone aren’t recommended for patients with cranial trauma who don’t require a corticosteroid for another conditions because of increased risk of death.

Triamcinolone should be administered with extreme caution, if at all, in patients who have active or quiescent tuberculosis infection of the respiratory tract, untreated fungal or bacterial infection, systemic viral or parasitic infection, or ocular herpes simplex because this drug can make these infections worse.

Give oral form of triamcinolone with meals to minimize GI distress.

Use calibrated device to measure liquid doses.

If necessary, crush tablets and mix with food or fluids.

Shake I.M. suspension thoroughly before drawing it into syringe.

Be aware that specialized training may be needed to administer parenteral triamcinolone.

Don’t administer parenteral forms of triamcinolone I.V.

Be aware that triamcinolone may reactivate tuberculosis in patients who have a history of it.

Monitor patients, especially infants, closely for gasping syndrome because parenteral triamcinolone contains benzyl alcohol. Exposure to high doses may result in toxicity evidenced by life-threatening hypotension and metabolic acidosis.
WARNING Assess patient for signs and symptoms of adrenal insufficiency (fatigue, hypotension, lassitude, nausea, vomiting, and weakness) during times of stress, such as infection, surgery, or trauma. Notify prescriber immediately if you detect these signs and symptoms because adrenal insufficiency may be lifethreatening.

Be aware that, although rare, bone mineral density loss and osteoporosis may occur, which may increase risk of fractures, especially in patients on prolonged triamcinolone therapy.

PATIENT SAFTY

Caution patient not to adjust triamcinolone dosage without consulting prescriber.

Teach patient how to administer nasal aerosols properly, using manufacturer’s instructions, to avoid nasal irritation.

Instruct patient to dispose of aerosol canister after 240 uses (100 uses for Nasacort HFA) because dosage may not be correct after that time.

Teach patient how to use
NASAL SPRAY, including how to prime spray pump bottle before use. Caution patient to not to get
NASAL SPRAY in eyes. If this occurs, patient should rinse his eyes well with water.

Inform patient that maximum benefit of triamcinolone therapy may not occur for up to 2 weeks.

Advise patient to notify prescriber immediately if asthma fails to respond to inhaled drug because additional systemic therapy may be needed.

Caution patient to avoid exposure to people who have chickenpox or measles throughout triamcinolone therapy and for 12 months afterward.

Advise patient to have periodic eye examinations during long-term therapy because triamcinolone can cause glaucoma or ocular nerve damage.

Category

Chemical class: Pterdine derivative
Therapeutic class: Diuretic

Pregnancy category: B

Indications

To treat edema in cirrhosis, heart failure, and nephrotic syndrome
Adults. Initial: 25 to 100 mg daily. Maximum: 300 mg daily.

Mechanism of Action

Inhibits sodium reabsorption in distal convoluted tubules and cortical collecting ducts, causing sodium and water loss and enhancing potassium retention.

Contraindications

Anuria, diabetic nephropathy or renal disease linked to renal insufficiency, hyperkalemia (potassium level of 5.5 mEq/L or more), hypersensitivity to triamterene or its components, severe hepatic dysfunction

Interactions

ACE inhibitors, amiloride, angiotensin-II receptor antagonists, cyclosporine, heparin, potassium-containing , potassium salts, potassium supplements, spironolactone: Increased risk of hyperkalemia amantadine: Decreased amantadine clearance, possibly amantadine toxicity antihypertensives: Increased antihypertensive effect diuretics: Increased diuretic effect folic acid: Possibly antagonized action of folic acid indomethacin: Increased risk of renal impairment lithium: Increased risk of lithium toxicity
NSAIDs: Decreased diuretic effect of triamterene, increased risk of hyperkalemia oral antidiabetic : Altered blood glucose control

Side Efect

CNS: Dizziness, fatigue, headache, weakness
EENT: Dry mouth
ENDO: Hyperglycemia, hypoglycemia
GI: Diarrhea, nausea, vomiting
GU: Azotemia, elevated BUN and serum creatinine levels, renal calculi
SKIN: Jaundice, photosensitivity, rash

Cautions

Be aware that triamterene shouldn’t be given to patient with creatinine clearance below 10 ml/min/1.73 m2because this condition increases the risk of druginduced hyperkalemia.

Monitor serum potassium level during therapy, especially in patient with renal impairment or diabetes mellitus. Also monitor patient’s BUN and serum creatinine levels to assess renal function and prevent hyperkalemia.

Monitor patient for irregular heartbeat, which is usually the first sign of hyperkalemia.

If you suspect hyperkalemia, obtain an ECG tracing, as ordered. A widened QRS complex or an arrhythmia requires prompt additional therapy.

Monitor laboratory test results and watch for signs of metabolic or respiratory acidosis, which may occur suddenly in patient with cardiac disease or uncontrolled diabetes mellitus.

Monitor patient’s serum uric acid and sodium levels, as ordered, because triamterene may reduce uric acid clearance and increase the risk of gout and hyperuricemia. This drug also may worsen preexisting hyponatremia.

Monitor CBC with differential because drug may increase the risk of megaloblastic anemia in patient with folic acid deficiency.

PATIENT SAFTY

Advise patient to take triamterene with food or milk.

Instruct patient to avoid exposure to excessive heat or sunlight to prevent dehydration and, possibly, photosensitivity.

Explain to patient with a history of gout that drug may increase the risk of attack.

Advise patient to notify prescriber about ineffective diuresis and unexplained weight gain during therapy.

Category

Chemical class: Benzodiazepine
Therapeutic class: Sedative-hypnotic

Pregnancy category: X

Controlled substance schedule: IV

Indications

To provide short-term management of insomnia
Adults. 0.125 to 0.25 mg at bedtime. Maximum: 0.5 mg daily (for patients with inadequate response to usual dose).
DOSAGE ADJUSTMENT For elderly or debilitated patients, initial dosage reduced to 0.125 mg at bedtime and maximum dosage limited to 0.25 mg daily.

Mechanism of Action

Potentiates effects of the inhibitory neurotransmitter gamma-aminobutyric acid, which increases inhibition of the ascending reticular activating system and produces varying levels of CNS depression, including sedation, hypnosis, skeletal muscle relaxation, anticonvulsant activity, and coma.

Contraindications

Hypersensitivity to triazolam or its components; itraconazole, ketoconazole, or nefazodone therapy; pregnancy

Interactions

anxiolytics, barbiturates, brompheniramine, carbinoxamine, cetirizine, chlorpheniramine, clemastine, cyproheptadine, dimenhydrinate, diphenhydramine, doxylamine, general anesthetics, methdilazine, opioid analgesics, sedative-hypnotics, phenothiazines, promethazine, tramadol, tricyclic antidepressants, trimeprazine: Increased sedation, respiratory depression cimetidine, diltiazem, disulfiram, erythromycin, probenecid, verapamil: Increased sedation fluconazole: Increased blood triazolam level and effects
flumazenil: Increased risk of withdrawal symptoms itraconazole, ketoconazole, nefazodone: Delayed triazolam elimination oral contraceptives: Increased blood triazolam level grapefruit juice: Increased blood triazolam level and sedation
alcohol use: Increased sedation, respiratory depression

Side Efect

CNS: Anxiety, ataxia, complex behaviors (such as sleep driving), confusion, depression, dizziness, drowsiness, fatigue, headache, insomnia, nightmares, syncope, talkativeness, tremor, vertigo
EENT: Throat tightness
GI: Nausea, vomiting
RESP: Dyspnea
Other: Anaphylaxis, angioedema, physical and psychological dependence

Cautions

Be aware that triazolam shouldn’t be discontinued abruptly, even after only 1 to 2 weeks of therapy. Doing so can cause withdrawal symptoms, including abdominal cramps, confusion, depression, diaphoresis, hyperacusis, insomnia, irritability, nausea, nervousness, paresthesia, perceptual disturbances, photophobia, tachycardia, tremor, and vomiting.
WARNING Assess patient for signs of physical and psychological dependence, and notify prescriber if they occur.

Monitor patient’s respiratory rate and depth and ABG results, as appropriate, because drug may worsen ventilatory failure in patient with pulmonary disease, such as severe COPD, respiratory depression, or sleep apnea. Use drug cautiously in patients with acute intermittent porphyria, myasthenia gravis, and severe renal impairment because it may aggravate these conditions.

Take safety precautions for elderly patients because triazolam may impair cognitive and motor function and increase the risk for falls.

Use drug cautiously in patients with advanced Parkinson’s disease because it may worsen cognition, coordination, and psychosis.
WARNING Monitor patient closely for hypersensitivity reactions such as dyspnea, throat tightness, nausea, vomiting, and swelling. If present, stop triazolam immediately, notify prescriber, and provide supportive care.

PATIENT SAFTY

Instruct patient to take triazolam exactly as prescribed and not to stop taking it abruptly because of the risk of having withdrawal symptoms.

Instruct patient to stop taking triazolam and seek emergency care if she has trouble breathing, throat tightness, nausea, vomiting, or abnormal swelling.

Advise patient that drug may cause abnormal behaviors during sleep, such as driving a car, eating, talking on the phone, or having sex without any recall of the event. If family notices any such behavior or patient sees evidence of such behavior upon awakening, the prescriber should be notified.

Caution patient about possible drowsiness during therapy.

Urge patient to avoid alcohol consumption because it increases drug’s sedative effects and risk of abnormal behaviors, such as sleep driving.

Advise patient to notify prescriber about excessive drowsiness, known or suspected pregnancy, and nausea.

Category

Chemical class: Piperazine phenothiazine
Therapeutic class: Antianxiety, antipsychotic

Pregnancy category: Not rated

Indications

To treat psychotic disorders SYRUP, Adults and adolescents. Initial: 2 to 5 mg b.i.d., increased gradually, as needed. Maintenance: 15 to 20 mg daily. Maximum: 40 mg daily. Children age 6 and over.Initial: 1 mg daily or in divided doses b.i.d., increased gradually, as needed.
I.M.INJECTION Adults and adolescents. 1 to 2 mg every 4 to 6 hr, as needed. Maximum: 10 mg daily. Children age 6 and over.1 mg daily or in divided doses b.i.d., as needed. To relieve anxiety SYRUP,,
I.M.INJECTION Adults and adolescents. Initial: 1 to 2 mg daily, increased gradually, as needed. Maximum: 6 mg daily for 12 wk.

Mechanism of Action

Blocks postsynaptic dopamine receptors, increasing dopamine turnover and decreasing dopamine neurotransmission. This action may depress the areas of the brain that control activity and aggression, including the cerebral cortex, hypothalamus, and limbic system. Trifluoperazine may relieve anxiety by indirectly reducing arousal and increasing the filtering of internal stimuli to the reticular activating system.

Contraindications

Blood dyscrasias; bone marrow depression; cerebral arteriosclerosis; coma; coronary artery disease; hepatic dysfunction; hypersensitivity to trifluoperazine, other phenothiazines, or their components; myeloproliferative disorders; severe hypertension or hypotension; significant CNS depression; subcortical brain damage; use of high doses of CNS depressants

Interactions

adsorbent antidiarrheals, aluminumand magnesium-containing antacids: Possibly inhibited absorption of oral trifluoperazine amantadine, anticholinergics, antidyskinetics, antihistamines: Possibly intensified adverse anticholinergic effects, increased risk of trifluoperazine-induced hyperpyrexia amphetamines: Decreased stimulant effect of amphetamines, decreased antipsychotic effect of trifluoperazine anticonvulsants: Lowered seizure threshold antithyroid : Increased risk of agranulocytosis apomorphine: Possibly decreased emetic response to apomorphine, additive CNS depression appetite suppressants: Decreased effects of appetite suppressants astemizole, cisapride, disopyramide, erythromycin, pimozide, probucol, procainamide,
quinidine: Prolonged QT interval, increased risk of ventricular tachycardia
beta blockers: Increased blood levels of both , possibly leading to additive hypotensive effect, arrhythmias, irreversible retinopathy, and tardive dyskinesia bromocriptine: Impaired therapeutic effects of bromocriptine
CNS depressants: Additive CNS depression ephedrine, metaraminol: Decreased vasopressor response to ephedrine epinephrine: Blocked alpha-adrenergic effects of epinephrine extrapyramidal reaction–causing (droperidol, haloperidol, metoclopramide, metyrosine, risperidone): Increased severity and frequency of extrapyramidal reactions hepatotoxic : Increased risk of hepatotoxicity hypotension-producing : Possibly severe hypotension with syncope levodopa: Decreased antidyskinetic effect of levodopa lithium: Reduced absorption of oral trifluoperazine, possibly encephalopathy and additive extrapyramidal effects MAO inhibitors, maprotiline, tricyclic antidepressants: Possibly prolonged and intensified sedative and anticholinergic effects, increased blood level of antidepressants, impaired trifluoperazine metabolism, increased risk of neuroleptic malignant syndrome mephentermine: Decreased antipsychotic effect of trifluoperazine and vasopressor effect of mephentermine methoxamine, phenylephrine: Decreased vasopressor effect and shortened duration of action of these metrizamide: Increased risk of seizures opioid analgesics: Increased risk of CNS and respiratory depression, orthostatic hypotension, severe constipation, and urine retention ototoxic : Possibly masking of some symptoms of ototoxicity, such as dizziness, tinnitus, and vertigo
phenytoin: Lowered seizure threshold; inhibited phenytoin metabolism, possibly leading to phenytoin toxicity photosensitizing : Possibly additive photosensitivity and intraocular photochemical damage to choroid, lens, or retina thiazide diuretics: Possibly hyponatremia and water intoxication
alcohol use: Increased CNS and respiratory depression, increased hypotensive effect

Side Efect

CNS: Akathisia, altered temperature regulation, dizziness, drowsiness, extrapyramidal reactions (dystonia, pseudoparkinsonism, tardive dyskinesia)
CV: Hypotension, orthostatic hypotension, tachycardia
EENT: Blurred vision, dry mouth, nasal congestion, ocular changes (deposits of fine particles in cornea and lens), pigmentary retinopathy
ENDO: Galactorrhea, gynecomastia
GI: Constipation, epigastric pain, nausea, vomiting
GU: Ejaculation disorders, menstrual irregularities, urine retention
SKIN: Contact dermatitis, decreased sweating, photosensitivity, pruritus, rash
Other: Injection site irritation and sterile abscess, weight gain

Cautions

WARNING Trifluoperazine shouldn’t be used to treat elderly patients with dementia-related psychosis because drug increases the risk of death in these patients

Use trifluoperazine cautiously in patients with glaucoma because of drug’s anticholinergic effect.

Before administration, observe parenteral solution, which may turn slightly yellow without altering its potency. Don’t use solution if discoloration is pronounced or precipitate is present.

For I.M. administration, inject drug slowly and deep into upper outer quadrant of the buttocks. Keep patient in a supine position for 30 minutes after injection to minimize hypotensive effect.

Rotate I.M. injection sites to avoid irritation and sterile abscesses.
WARNING Watch closely for tardive dyskinesia, which may continue after treatment stops. Signs include uncontrolled movements of arms, body, cheeks, jaw, legs, mouth, or tongue. Notify prescriber if such signs occur.

Closely monitor elderly patients and severely ill or dehydrated children. They’re at increased risk for certain adverse CNS reactions.

To prevent contact dermatitis, avoid skin contact with oral or injection solution.

PATIENT SAFTY

Instruct patient to take trifluoperazine exactly as prescribed and not to stop taking drug abruptly or without consulting prescriber.

Advise patient to take drug with food or a full glass of milk or water to minimize adverse GI reactions.

Urge patient to consult prescriber before using other because of possible interactions.

Instruct patient to notify prescriber immediately if she experiences difficulty swallowing or speaking and her tongue protrudes from her mouth.

Caution patient to avoid alcohol during therapy.

Advise patient to avoid potentially hazardous activities until drug’s CNS effects are known.

Instruct patient to change position slowly to minimize effects of orthostatic hypotension.

Urge patient to avoid exposure to the sun and extreme heat because drug may cause photosensitivity and interfere with thermoregulation. Encourage her to wear sunscreen when outdoors.

Category

Chemical class: Phenothiazine
Therapeutic class: Antiemetic, antipsychotic

Pregnancy category: Not rated

Indications

To treat psychotic disorders
I.M.INJECTION Adults and adolescents. 60 mg, as needed. Maximum: 150 mg daily. Children age 30 months and over.0.2 to 0.25 mg/kg, as needed. Maximum: 10 mg daily. To treat nausea and vomiting
I.V.INJECTION
Adults. 1 mg, p.r.n. Maximum: 3 mg daily.
I.M.INJECTION Adults and adolescents. 5 to 15 mg every 4 hr. Maximum: 60 mg daily. Children age 30 months and over. 0.2 to 0.25 mg/kg, p.r.n. Maximum: 10 mg daily.

Mechanism of Action

Blocks postsynaptic dopamine receptors, increasing dopamine turnover and decreasing dopamine neurotransmission. This action may depress the areas of the brain that control activity and aggression, including the cerebral cortex, hypothalamus, and limbic system. Triflupromazine also prevents nausea and vomiting by inhibiting or blocking dopamine receptors in the medullary chemoreceptor trigger zone and, peripherally, by blocking the vagus nerve in the GI tract.

Contraindications

Blood dyscrasias, bone marrow depression, cerebral arteriosclerosis, coma or severe CNS depression, concurrent use of large amount of CNS depressants, coronary artery disease, hepatic dysfunction, hypersensitivity to phenothiazines, severe hypertension or hypotension, subcortical brain damage

Interactions

amantadine, anticholinergics, antidyskinetics, antihistamines: Possibly intensified adverse anticholinergic effects and increased risk of triflupromazine-induced hyperpyrexia amphetamines: Decreased stimulant effect of amphetamines, decreased antipsychotic effect of triflupromazine anticonvulsants: Lowered seizure threshold antithyroid : Increased risk of agranulocytosis apomorphine: Possibly decreased emetic response to apomorphine, additive CNS depression appetite suppressants: Decreased anorectic effect of appetite suppressants astemizole, cisapride, disopyramide, erythromycin, pimozide, probucol, procainamide,
quinidine: Prolonged QT interval, increased risk of ventricular tachycardia
beta blockers: Increased blood levels of both , possibly leading to additive hypotensive effect, arrhythmias, irreversible retinopathy, and tardive dyskinesia bromocriptine: Impaired therapeutic effects of bromocriptine
CNS depressants: Additive CNS depressant effects ephedrine: Decreased vasopressor response to ephedrine epinephrine: Blocked alpha-adrenergic effects of epinephrine extrapyramidal reaction–causing (droperidol, haloperidol, metoclopramide, metyrosine, risperidone): Increased severity and frequency of extrapyramidal reactions hepatotoxic : Increased risk of hepatotoxicity hypotension-producing : Possibly severe hypotension with syncope levodopa: Decreased antidyskinetic effect of levodopa lithium: Possibly encephalopathy and additive extrapyramidal effects MAO inhibitors, maprotiline, tricyclic antidepressants: Increased CNS depression, impaired triflupromazine metabolism, increased risk of neuroleptic malignant syndrome mephentermine: Possibly antagonized antipsychotic effect of triflupromazine and vasopressor effect of mephentermine metaraminol: Decreased vasopressor effect of metaraminol methoxamine, phenylephrine: Decreased vasopressor effect and shortened duration of action of these metrizamide: Increased risk of seizures opioid analgesics: Increased risk of CNS and respiratory depression, orthostatic hypotension, severe constipation, and urine retention ototoxic : Possibly masking of symptoms of ototoxicity, such as dizziness, tinnitus, and vertigo
phenytoin: Lowered seizure threshold; inhibited phenytoin metabolism, possibly leading to phenytoin toxicity photosensitizing : Possibly additive photosensitivity and intraocular photochemical damage to choroid, lens, or retina thiazide diuretics: Possibly hyponatremia and water intoxication
alcohol use: Increased CNS and respiratory depression, increased hypotensive effect

Side Efect

CNS: Akathisia, altered temperature regulation, dizziness, drowsiness, extrapyramidal reactions (dystonia, pseudoparkinsonism, tardive dyskinesia)
CV: Hypotension, orthostatic hypotension, tachycardia
EENT: Blurred vision, dry mouth, nasal congestion, ocular changes (deposits of fine particles in cornea and lens), pigmentary retinopathy
ENDO: Galactorrhea, gynecomastia
GI: Constipation, epigastric pain, nausea, vomiting
GU: Ejaculation disorders, menstrual irregularities, urine retention
SKIN: Decreased sweating, photosensitivity, pruritus, rash
Other: Injection site irritation and sterile abscess, weight gain

Cautions

Use triflupromazine cautiously in patients with glaucoma because of drug’s anticholinergic effects.

Before administration, observe parenteral solution, which may turn slightly yellow without altering potency. Don’t use solution if discoloration is pronounced or precipitate is present.

Don’t let solution come in contact with your skin because contact dermatitis may occur.

For I.M. administration, slowly inject triflupromazine deep into upper outer quadrant of buttocks. Keep patient supine for 30 minutes afterward to minimize hypotensive effect.

Rotate I.M. injection sites to avoid irritation and sterile abscesses.
WARNING Watch closely for tardive dyskinesia, which may continue after treatment stops. Signs include uncontrolled movements of arms, body, cheeks, jaw, legs, mouth, or tongue. Notify prescriber if such signs occur.

Closely monitor elderly patients and severely ill or dehydrated children. They’re at increased risk for certain adverse CNS reactions.

PATIENT SAFTY

Instruct patient to change position slowly to minimize effects of orthostatic hypotension.

Urge patient to avoid potentially hazardous activities until triflupromazine’s CNS effects are known.

Instruct patient to notify prescriber immediately if she experiences difficulty swallowing or speaking and her tongue protrudes from her mouth.

Caution patient to avoid alcohol during therapy.

Urge patient to avoid exposure to the sun and extreme heat because drug may cause photosensitivity and interfere with thermoregulation. Encourage her to wear sunscreen when outdoors.

Category

Chemical class: Tertiary amine
Therapeutic class: Antidyskinetic

Pregnancy category: C

Indications

To treat parkinsonism ELIXIR,
Adults. Initial: 1 to 2 mg on day 1, divided into 3 equal doses and given with meals. Total daily dose increased by 2 mg every 3 to 5 days until desired response or maximum dose is reached. Maximum: 15 mg daily.
Adults. 5 mg after breakfast; additional 5 mg 12 hr later, if needed. Maximum: 15 mg daily. To treat drug-induced extrapyramidal symptoms
Adults. 1 mg daily, increased to 5 to 15 mg/ day, as prescribed, to control symptoms.

Mechanism of Action

Blocks acetylcholine’s action at cholinergic receptor sites, which restores normal dopamine and acetylcholine balance in the brain, relaxing muscle movement and decreasing drooling, rigidity, and tremor. Drug also may inhibit reuptake and storage of dopamine, prolonging its action.

Contraindications

Achalasia, bladder neck or prostatic obstruction, narrow-angle glaucoma, hypersensitivity to trihexyphenidyl or its components, megacolon, myasthenia gravis, pyloric or duodenal obstruction, stenosing peptic ulcer

Interactions

amantadine, anticholinergics, MAO inhibitors, tricyclic antidepressants: Increased anticholinergic effects antidiarrheals (adsorbent): Possibly decreased therapeutic effects of trihexyphenidyl chlorpromazine: Decreased blood chlorpromazine level
CNS depressants: Increased sedative effect levodopa: Increased efficacy of levodopa
alcohol use: Increased sedation

Side Efect

CNS: Confusion, dizziness, drowsiness, nervousness
EENT: Blurred vision; dry eyes, mouth, nose, or throat; mydriasis
GI: Constipation, nausea, vomiting
GU: Dysuria, urine retention
SKIN: Decreased sweating

Cautions

Use trihexyphenidyl cautiously in patients with cardiovascular, hepatic, or renal disorders. Patients with cardiovascular disorders, such as atherosclerosis, hypertension, and ischemic heart disease, are at risk for tachycardia and coronary ischemia from drug’s positive chronotropic effects. Hepatic and renal dysfunction increase the risk of

Side Efect

.

Before therapy begins, assess patient’s muscle rigidity and tremor to establish a baseline. During therapy, reassess patient to detect improvement in these signs and evaluate drug effectiveness.

Obtain patient’s intraocular pressure before and periodically during trihexyphenidyl therapy, as ordered, because drug can precipitate incipient glaucoma.

PATIENT SAFTY

Instruct patient to take trihexyphenidyl after meals.

Teach patient not to break or chew capsules.

Instruct patient to use calibrated device to measure elixir.

Advise patient to avoid potentially hazardous activities until drug’s CNS effects are known.

Advise patient with dry eyes or increased contact lens awareness to use lubricating drops or stop wearing contact lenses during drug therapy.

Caution patient being treated for parkinsonism not to stop taking trihexyphenidyl suddenly because doing so may worsen symptoms.

Advise patient to maintain adequate hydration and avoid exercising during hot weather because trihexyphenidyl increases the risk of heatstroke.

Category

Chemical class: Ethanolamine derivative
Therapeutic class: Antiemetic

Pregnancy category: Not rated

Indications

To treat nausea and vomiting Adults and adolescents. 250 mg every 6 to 8 hr, p.r.n. Children weighing 15 to 45 kg (33 to 99 lb). 100 to 200 mg every 6 to 8 hr, p.r.n. I.M.INJECTION Adults and adolescents. 200 mg every 6 to 8 hr, p.r.n.
DOSAGE ADJUSTMENT For patient with renal impairment, dosage decreased or dose interval lengthened.

Mechanism of Action

Prevents or stops nausea and vomiting by blocking dopamine receptors and emetic impulses at the chemoreceptor trigger zone in the brain.

Contraindications

Children (I.M.); hypersensitivity to trimetho-benzamide, benzocaine, or any of their components

Interactions

apomorphine: Decreased emetic response to apomorphine, increased CNS effects barbiturates, belladonna alkaloids, phenothiazines: Increased risk of coma, extrapyramidal reactions, opisthotonos, and seizures
CNS depressants: Possibly enhanced effects of both ototoxic : Possibly masked signs of ototoxicity

Side Efect

CNS: Dizziness, drowsiness, headache
EENT: Blurred vision
GI: Diarrhea
MS: Muscle cramps
Other: Injection site burning, irritation, pain, redness, or swelling

Cautions

Use trimethobenzamide cautiously in dehydrated patients and those with an electrolyte imbalance, encephalitis, encephalopathy, gastroenteritis, or high fever.

Be aware that trimethobenzamide shouldn’t be used in children who have viral illnesses because they’re at increased risk for Reye’s syndrome, characterized by abrupt onset of irrational behavior; lethargy; persistent, severe vomiting; progressive encephalopathy leading to coma, seizures, and possibly death.

To minimize injection site irritation, inject trimethobenzamide deep into a large muscle mass using the Z-track technique, which blocks solution from escaping along the injection route.

PATIENT SAFTY

Inform patient that drug may cause blurred vision, dizziness, and drowsiness. Advise her to avoid hazardous activities until drug’s CNS effects are known.

Inform patient’s parents or caregivers that trimethobenzamide may cause Reye’s syndrome, and urge them to notify prescriber immediately if they notice decreased level of consciousness, irrational behavior, lethargy, or severe vomiting.

Category

Chemical class: Dihydrofolic acid analogue
Therapeutic class: Antibiotic

Pregnancy category: C

Indications

To treat UTI caused by Enterobacter species, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, or coagulase-negative staphylococci, including Staphylococcus saprophyticus Adults and children age 12 and over. 100 mg every 12 hr or 200 mg daily for 10 days.
DOSAGE ADJUSTMENT For patients with creatinine clearance of 15 to 30 ml/min/ 1.73 m2, dosage usually reduced by 50%.

Mechanism of Action

Inhibits formation of tetrahydrofolic acid, the metabolically active form of folic acid, in susceptible bacteria. This depletes folate, an essential component of bacterial development, thereby disrupting production of bacterial nucleic acid and protein.

Contraindications

Hypersensitivity to trimethoprim or its components, megaloblastic anemia from folate deficiency, severe renal impairment (creatinine clearance less than 15 ml/min/ 1.73 m2)

Interactions

bone marrow depressants: Increased risk of leukopenia, thrombocytopenia cyclosporine: Increased risk of nephrotoxicity dapsone: Increased blood levels and risk of adverse effects (especially methemoglobinemia) of both folate antagonists: Increased risk of megaloblastic anemia
phenytoin: Decreased phenytoin metabolism, increased risk of phenytoin toxicity procainamide: Increased blood levels of procainamide and its metabolite, N-acetylprocainamide
rifampin: Increased elimination and decreased effectiveness of trimethoprim
warfarin: Increased anticoagulant activity of warfarin

Side Efect

CNS: Fever, headache
EENT: Glossitis
GI: Abdominal pain, anorexia, diarrhea, elevated liver function test results, epigastric pain, nausea, vomiting
GU: Elevated BUN and serum creatinine levels
HEME: Leukopenia, megaloblastic anemia, methemoglobinemia, neutropenia, thrombocytopenia
SKIN: Exfoliative dermatitis, pruritus, rash

Cautions

Obtain urine specimen, as ordered, before trimethoprim therapy starts.

Give drug on an empty stomach to enhance absorption.

Evaluate patient’s test values for folic acid deficiency and signs of bone marrow depression.

Monitor serum potassium level and renal function studies, as ordered, in patients with decreased renal function because these patients are at increased risk for hyperkalemia and toxic reactions when receiving trimethoprim.

PATIENT SAFTY

Instruct patient to complete entire course of trimethoprim therapy, as prescribed, even if she feels better beforehand.

Advise patient to take drug with food or milk if GI distress occurs.

Instruct patient to notify prescriber if she experiences rash, severe fatigue, sore throat, or unusual bleeding or bruising.

Category

Chemical class: Dibenzazepine derivative
Therapeutic class: Antidepressant

Pregnancy category: C

Indications

To treat depression Adults in inpatient settings.Initial: 100 mg daily in divided doses, increased gradually in a few days to 200 mg daily. Maximum: 300 mg daily in 2 to 3 wk. Adolescents in inpatient settings. Initial: 50 mg daily in divided doses, increased as needed. Maximum: 100 mg daily. Adults in outpatient settings. Initial: 75 mg/day in divided doses, increased gradually up to 150 mg daily, as needed. Maintenance: 50 to 150 mg daily. Maximum: 200 mg daily. Adolescents in outpatient settings. Initial: 50 mg daily in divided doses, increased as needed. Maximum: 100 mg daily.
DOSAGE ADJUSTMENT For elderly patients, initial dosage reduced to 50 mg daily in divided doses, and maximum dosage limited to 100 mg daily.

Mechanism of Action

Inhibits the reuptake of norepinephrine at presynaptic neurons, thus increasing its concentration in synapses. This action may elevate mood and relieve depression.

Contraindications

Hypersensitivity to trimipramine, other dibenzazepine tricyclic antidepressants, or their components; recovery period after an MI; use within 14 days of an MAO inhibitor or other tricyclic antidepressant

Interactions

amantadine, anticholinergics, antidyskinetics, antihistamines: Increased anticholinergic effects (confusion, hallucinations, nightmares) anticonvulsants: Increased CNS depression, lowered seizure threshold (high trimipramine doses), decreased anticonvulsant effect antithyroid : Risk of agranulocytosis barbiturates, carbamazepine: Decreased blood level and effects of trimipramine bupropion, clozapine, cyclobenzaprine, haloperidol, loxapine, maprotiline, molindone, phenothiazines,
thioxanthenes: Increased and prolonged sedative and anticholinergic effects of both , increased risk of seizures
cimetidine: Decreased trimipramine metabolism, possibly leading to trimipramine toxicity
clonidine: Decreased hypotensive effect and increased CNS depressant effect of clonidine
CNS depressants: Increased hypotension and CNS and respiratory depression disulfiram, ethchlorvynol: Transient delirium, risk of CNS depression (ethchlorvynol) fluoxetine: Increased trimipramine level guanadrel, guanethidine: Decreased hypotensive effect
MAO inhibitors: Increased risk of death, hyperpyrexia, hypertensive crisis, severe seizures
methylphenidate: Decreased methylphenidate effects, increased blood trimipramine level metrizamide: Increased risk of seizures naphazoline (ophthalmic), oxymetazoline (nasal or ophthalmic), phenylephrine (nasal or ophthalmic), xylometazoline (nasal): Increased vasopressor effect of these oral anticoagulants: Increased anticoagulation phenothiazines: Increased blood trimipramine level, decreased phenothiazine metabolism pimozide, probucol: Increased risk of arrhythmias, possibly prolonged QT interval sympathomimetics: Increased risk of arrhythmias, hyperpyrexia, severe hypertension thyroid hormones: Increased therapeutic and toxic effects of both
alcohol use: Increased hypotension and CNS and respiratory depression

Side Efect

CNS: Anxiety, ataxia, confusion, delirium, dizziness, drowsiness, excitement, extrapyramidal reactions, hallucinations, headache, insomnia, nervousness, nightmares, parkinsonism, seizures, stroke, suicidal ideation, tremor
CV: Arrhythmias, orthostatic hypotension
EENT: Blurred vision, dry mouth, increased intraocular pressure, taste perversion, tinnitus, tongue swelling
ENDO: Gynecomastia, syndrome of inappropriate ADH secretion
GI: Constipation, diarrhea, heartburn, ileus, increased appetite, nausea, vomiting
GU: Sexual dysfunction, testicular swelling, urine retention
HEME: Agranulocytosis, bone marrow depression
RESP: Wheezing
SKIN: Alopecia, diaphoresis, jaundice, photosensitivity, pruritus, rash, urticaria
Other: Facial edema, weight gain

Cautions

Watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes and particularly if patient is a child, teenager, or young adult.

Expect to gradually reduce trimipramine dosage, as prescribed, before electroconvulsive therapy.

PATIENT SAFTY

Instruct patient to take the last dose early in the evening to avoid insomnia.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Urge patient to change position slowly to minimize orthostatic hypotension.

Urge patient to avoid alcohol during therapy.

Advise patient to avoid exposure to excessive sunlight and to wear sunscreen when she’s outdoors.

Instruct patient to notify prescriber about the development of unusual bruising and signs of infection.

Suggest that patient use sugarless gum or hard candy to relieve dry mouth.
WARNING Urge parents to watch their child or adolescent closely for abnormal behavior, increased aggression or hostility, or suicidal tendencies, especially when therapy starts or dosage is adjusted. Stress need to notify prescriber about changes.

Category

Chemical class: Organic amine
Therapeutic class: Alkalinizer

Pregnancy category: C

Indications

To treat metabolic acidosis associated with cardiac arrest
IV: Adults and children. 3.6 to 10.8 g (111 to 333 ml) of 0.3 M solution. I.V.INJECTION Adults and children. If chest is opened, 2 to 6 g injected directly into open ventricular cavity. To treat metabolic acidosis during cardiac bypass surgery
IV: Adults and children. 9 ml (2.7 mEq or 0.32 g) of 0.3 M solution/kg as a single dose. Usual: 500 ml (150 mEq or 18 g) infused over 1 hr. Maximum: 500 mg/kg over 1 hr.

Mechanism of Action

Combines with hydrogen ions and their associated acid anions, including lactic, pyruvic, and carbonic acid, to form salts that are excreted in urine. Tromethamine exerts additional alkalinizing effects by acting as an osmotic diuretic, promoting the excretion of alkaline urine that contains increased amounts of carbon dioxide and electrolytes.

Contraindications

Anuria, chronic respiratory acidosis, hypersensitivity to tromethamine or its components, uremia

Interactions

amphetamines, quinidine, other pHdependent : Altered excretion of these

Side Efect

CNS: Fever
CV: Vasospasm
ENDO: Hypoglycemia
GI: Hepatic necrosis (hemorrhagic)
RESP: Respiratory depression
Other: Hypervolemia; infusion site infection, phlebitis, or venous thrombosis; metabolic alkalosis

Cautions

Evaluate blood pH, blood glucose, and serum bicarbonate and electrolyte levels, and partial pressure of arterial carbon dioxide before, during, and after tromethamine therapy, as ordered.

Be aware that, except in life-threatening situations, tromethamine therapy is limited to no more than 1 day because of the risk of alkalosis.
WARNING Be aware that exceeding the recommended dosage can cause alkalosis, respiratory depression, and reduced carbon dioxide level.

Expect I.V. tromethamine administration to increase the risk of hypervolemia and pulmonary edema.

Assess the infusion site often for infiltration, which may cause inflammation, necrosis, thrombosis, tissue sloughing, and vasospasm.

Be aware that patients with renal failure have an increased risk of developing hyperkalemia. For such patients, be prepared to monitor ECG continuously and assess serum potassium level frequently.

Monitor patient’s blood glucose level often during and after therapy because rapid delivery can cause hypoglycemia for several hours.

PATIENT SAFTY

Inform family members that patient’s vital signs and laboratory test results will be measured frequently to monitor her progress.

Category

Chemical class: Quaternary ammonium compound
Therapeutic class: Bladder antispasmodic

Pregnancy category: C

Indications

To treat overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency
Adults. 20 mg b.i.d. 1 hour before meals or on empty stomach.
DOSAGE ADJUSTMENT For patients with severe renal insufficiency (creatinine clearance less than 30 ml/min/1.73 m2) and patients age 75 or over, dosage reduced to 20 mg daily at bedtime.
Adults. 60 mg daily in the morning, 1 hour before a meal or on empty stomach.

Mechanism of Action

Antagonizes the effect of acetylcholine on muscarinic receptors in the bladder. Trospium’s parasympatholytic action reduces the tonus of smooth muscle in the bladder. These actions increase maximum cystometric bladder capacity and volume with the first detrusor contraction, which relieves the sensation of urgency and frequency and enhances bladder control.

Contraindications

Gastric retention, hypersensitivity to trospium or its components, uncontrolled angleclosure glaucoma, urine retention

Interactions

anticholinergics: Increased frequency or severity of adverse effects; possibly reduced absorption of trospium digoxin, metformin, morphine, pancuronium, procainamide: Possibly increased plasma concentration of trospium, digoxin, metformin, morphine, pancuronium, procainamide
alcohol use: Possibly increased drowsiness

Side Efect

CNS: Dizziness, drowsiness, fatigue, headache, light-headedness
CV: Palpitations, tachycardia
EENT: Blurred vision; dry eyes, mouth, or throat
GI: Abdominal distention or pain, constipation, flatulence, indigestion, vomiting
GU: Urine retention
SKIN: Decreased sweating, dry skin, flushing, rash
Other: Angioedema

Cautions

Use trospium cautiously in patients with ulcerative colitis, intestinal atony, or myasthenia gravis because drug may decrease GI motility; patients with significant bladder outflow obstruction because drug may cause urine retention; patients with hepatic impairment because drug’s effects on the liver are unknown; and patients with renal impairment because drug excretion may be impaired.

Monitor elderly patients carefully, especially those age 75 or over, for adverse reactions because elderly patients have an increased risk of trospium-induced

Side Efect

.

PATIENT SAFTY

Instruct patient to take trospium on an empty stomach or at least 1 hour before eating because food delays its absorption.

Caution patient to avoid performing activities in a warm or hot environment because sweating may be delayed, which could cause a sudden increase in body temperature and heatstroke.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Inform patient that alcohol may increase the risk of drowsiness; urge patient to limit or abstain from alcoholic beverages while taking trospium.

Category

Chemical class: Isoquinoline derivative
Therapeutic class: Anticonvulsant

Pregnancy category: C

Indications

To manage muscle contractions of seizures associated with electroshock therapy I.V.INJECTION
Adults. 157 mcg/kg (0.157 mg/kg) over 30 to 90 sec, given just before electroshock therapy. Expect initial dose to be 3 mg less than calculated total dose. To produce skeletal muscle paralysis during anesthesia I.V.OR
I.M.INJECTION
Adults. Initial: 6 to 9 mg. Maintenance: 3 to 4.5 mg in 3 to 5 min. if needed. For prolonged procedures, 3-mg supplemental doses given. Infants and children.500 mcg/kg I.V. Neonates.Initial: 250 to 500 mcg/kg I.V. Maintenance: One-fifth to one-sixth of initial dose if needed. To facilitate endotracheal intubation and aid controlled respiration during mechanical ventilation

Mechanism of Action

Tubocurarine reduces the intensity of skeletal muscle contractions caused by electrically induced seizures. Normally, when a nerve impulse arrives at a somatic motor nerve terminal, it triggers acetylcholine (ACh) stored in synaptic vesicles to be released into the neuromuscular junction. The released ACh binds with nicotinic receptors embedded in the skeletal muscle motor endplate, as shown below left, triggering muscle cell depolarization and contraction. Tubocurarine is a nondepolarizing neuromuscular blocker that acts as a competitive antagonist of ACh.By binding to the nicotinic receptors,as shown below right,it prevents transmission of the action potential at the neuromuscular junction,thereby sustaining skeletal muscle relaxation and eliminating the peripheral muscular manifestations of seizures.The drug has no effect on the CNS processes involved with seizures because it doesn’t cross the bloodbrain barrier.
Adults. Initial: 16.5 mcg/kg. Maintenance: Dosage individualized based on patient response. To aid in the diagnosis of myasthenia gravis
I.V.INJECTION
Adults. 4 to 33 mcg/kg. After 2 to 3 min, 1.5 mg of neostigmine is given I.V. to terminate the test.

Incompatibilities

Don’t mix tubocurarine with barbiturates, such as methohexital or thiopental, because a precipitate may form.

Contraindications

Hypersensitivity to tubocurarine or its components, patients in whom histamine release may be dangerous

Interactions

alfentanil, fentanyl, sufentanil: Prevented or reversed muscle rigidity from these aminoglycosides, anesthetics, capreomycin, citrate-anticoagulated blood, clindamycin, lidocaine (I.V.), lincomycin, polymyxins, procaine (I.V.), trimethaphan: Additive neuromuscular blocking effects beta blockers, calcium salts: Prolonged and enhanced effects of tubocurarine magnesium salts, procainamide,
quinidine: Enhanced blockade effects opioid analgesics: Additive histamine release effects, additive respiratory depressant effects, worsened bradycardia and hypotension

Side Efect

CV: Arrhythmias, bradycardia, edema, hypotension, shock, tachycardia
RESP: Bronchospasm
SKIN: Erythema, flushing, itching, rash
Other: Anaphylaxis

Cautions

If patient has a history of CV disease or is hypotensive, monitor her for further decrease in blood pressure.

Monitor patient for bronchospasm and hypotension because tubocurarine may cause increased histamine release.

Keep emergency equipment and readily available in case respiratory depression occurs.

PATIENT SAFTY

Explain the need for frequent hemodynamic monitoring.

Category

Chemical class: Carbonic acid diamide salt
Therapeutic class: Antiglaucoma, diuretic

Pregnancy category: C

Indications

To reduce cerebral edema and intracranial pressure
IV: Adults and children age 2 and over. 500 mg to 1.5 g/kg as 30% solution in D5W, D10W, or 10% invert sugar solution infused over 30 min to 2 hr at 4 or 6 ml/min, according to manufacturer’s instructions. Maximum: 2 g/kg daily. Children under age 2. 100 mg to 1.5 g/kg as 30% solution in D5W, D10W, or 10% invert sugar solution infused over 30 min to 2 hr at 4 or 6 ml/min, according to manufacturer’s instructions. To treat malignant or secondary glaucoma
IV:
Adults.500 mg to 1.5 g/kg as 30% solution in D5W, D10W, or 10% invert sugar solution infused over 30 min to 2 hr at 4 or 6 ml/min, according to manufacturer’s instructions. Maximum: 2 g/kg daily.
DOSAGE ADJUSTMENT Dosage reduced or drug withheld for patients with renal impairment if BUN level rises to 75 mg/dl or more or if diuresis fails to occur within 2 hr after administration.

Mechanism of Action

Elevates blood plasma osmolality, creating an osmotic effect that increases movement of water from the brain, CSF, and anterior portion of the eyes into interstitial fluid and plasma. This action reduces cerebral edema, intracranial pressure, CSF volume, and intraocular pressure. Large doses inhibit reabsorption of water and solutes in the renal tubules and induce diuresis by affecting the osmotic pressure gradient of the glomerular filtrate.

Contraindications

Active intracranial bleeding, hepatic failure, hypersensitivity to urea or its components, renal impairment, severe dehydration

Interactions

carbonic anhydrase inhibitors, other diuretics: Additive diuretic and intraocular pressure– reducing effects lithium: Increased renal excretion of lithium

Side Efect

CNS: Agitation, confusion, fever, headache, hyperthermia, nervousness, subarachnoid hemorrhage, subdural hematoma, syncope
CV: Tachycardia
EENT: Dry mouth, intraocular hemorrhage
GI: Nausea, thirst, vomiting
GU: Elevated BUN level
HEME: Hemolysis
SKIN: Blemishes, extravasation with tissue necrosis and sloughing
Other: Dehydration, hypokalemia, hyponatremia, infusion site phlebitis or thrombosis

Cautions

For maximum reduction of intracranial or intraocular pressure, expect to give urea 60 minutes before ocular or intracranial surgery.

Don’t mix urea with invert sugar solution if patient has fructose intolerance from aldolase deficiency.

Avoid infusing drug into leg veins to reduce risk of phlebitis and thrombosis.

Discard unused portion of drug after 24 hours.

Be aware that rapid administration may cause hemolysis, increased capillary bleeding, and, in patients with glaucoma, intraocular hemorrhage.

Maintain adequate hydration to minimize

Side Efect

. Assess for signs of dehydration, including dry mucous membranes and tenting.

Monitor BUN and serum electrolyte levels as well as fluid intake and output during urea therapy because prolonged use can cause diuresis.

PATIENT SAFTY

Instruct patient to notify prescriber immediately about difficulty breathing or shortness of breath because drug can cause transient increases in circulatory volume, leading to circulatory overload, worsening of heart failure, or pulmonary edema.

Tell patient to expect increased urine output.

Encourage patient to remain on bed rest during therapy.

Category

Chemical class: Renal enzymatic protein
Therapeutic class: Thrombolytic

Pregnancy category: B

Indications

To treat acute coronary artery thrombosis INTRACORONARY INFUSION
Adults.6,000 international units/min until artery is maximally opened (up to 2 hr may be required). Usual: 500,000 international units. To treat acute pulmonary thromboembolism including massive events
IV:
Adults. Initial: 4,400 international units/kg over 10 min, followed by 4,400 international units/kg/hr for 12 hr. To clear I.V. catheter occlusion Adults and children.5,000 international units/ml instilled into occluded line.

Mechanism of Action

Indirectly promotes conversion of plasminogen to plasmin, an enzyme that breaks down fibrin clots, fibrinogen, and other plasma proteins, including procoagulant factors V and VIII.

Incompatibilities

Don’t administer I.V. urokinase through same I.V. line as other or add other to urokinase solution.

Contraindications

Arteriovenous malformation, bleeding disorder, hypersensitivity to urokinase or its components, internal bleeding, intracranial aneurysm, intracranial or intraspinal surgery during previous 2 months, intracranial tumor, recent cardiopulmonary resuscitation, recent trauma, severe uncontrolled hypertension (systolic blood pressure 200 mm Hg or higher, or diastolic blood pressure 110 mm Hg or higher), stroke during previous 2 months

Interactions

antifibrinolytics (aminocaproic acid, aprotinin): Mutual antagonism antihypertensives: Increased risk of severe hypotension cefamandole, cefoperazone, cefotetan, plicamycin,
valproic acid: Increased risk of hypoprothrombinemia and severe hemorrhage corticosteroids, ethacrynic acid, salicylates (nonacetylated): Increased risk of GI ulceration and bleeding enoxaparin, heparin, NSAIDs, oral anticoagulants, platelet-aggregation inhibitors: Increased risk of hemorrhage thiotepa: Increased therapeutic effects of thiotepa

Side Efect

CNS: Chills, CVA, fever, headache
CV: Arrhythmias, including tachycardia; chest pain; cholesterol embolization; hypertension; hypotension
EENT: Orolingual edema
GI: Nausea, vomiting
HEME: Unusual bleeding
MS: Back pain, myalgia
RESP: Bronchospasm, dyspnea, hypoxemia, wheezing
SKIN: Cyanosis, ecchymosis, flushing, pruritus, rash, urticaria
Other: Anaphylaxis, infusion site reactions, metabolic acidosis

Cautions

To prevent foaming, don’t shake urokinase when reconstituting. Consult pharmacist about giving drug through 0.45-micron or smaller cellulose membrane filter.

Assess baseline hematocrit, platelet count, thrombin time, APTT, PT, and INR as ordered.

Monitor heart rate and rhythm by continuous ECG during therapy, especially during rapid lysis of coronary thrombi. Arrhythmias can occur with reperfusion.

Monitor blood pressure for hypotension. If it occurs, notify prescriber and expect to reduce infusion rate.

Check for bleeding at puncture sites and in urine and stool. Check for intracranial bleeding by performing frequent neurologic assessments.

After arterial puncture, apply pressure for at least 30 minutes and then apply pressure dressing. Check often for bleeding during therapy.

To prevent bleeding and associated complications, avoid venipunctures; use an external blood pressure cuff to measure blood pressure; give acetaminophen (not aspirin), as prescribed, for fever; and handle patient as little as possible.
WARNING If serious bleeding begins and can’t be controlled with local pressure, stop infusion immediately and notify prescriber.

PATIENT SAFTY

Instruct patient to remain on bed rest during urokinase therapy.

Inform patient that minor bleeding may occur at wounds or puncture sites.

Category

Chemical class: Naturally occurring bile acid
Therapeutic class: Bile salt replenisher, cholelitholytic

Pregnancy category: B

Indications

To prevent gallstone formation in obese patients during rapid weight loss Adults and adolescents.300 mg b.i.d. Or, 8 to 10 mg/kg daily in divided doses b.i.d or t.i.d. To dissolve gallstones Adults and adolescents.8 to 10 mg/kg daily in divided doses b.i.d. or t.i.d. To treat primary biliary cirrhosis
Adults.13 to 15 mg/kg daily in two to four divided doses.

Mechanism of Action

Suppresses hepatic synthesis, biliary secretion, and intestinal reabsorption of cholesterol. Prolonged use promotes dissolution of gallstones.

Contraindications

Acute cholangiitis; gallstone complications (such as biliary GI fistula; biliary obstruction; calcified, radiopaque, or radiotranslucent bile-pigment gallstones; cholecystitis; pancreatitis); hypersensitivity to ursodiol, other bile acids, or their components

Interactions

aluminum-containing antacids, cholestyramine, colestipol: Decreased absorption and therapeutic effects of ursodiol clofibrate, estrogens, neomycin, oral contraceptives, progestins: Interference with ursodiol’s therapeutic effects; increased risk of gallstone formation any : Increased dissolution of drug

Side Efect

CNS: Anxiety, asthenia, depression, fatigue, headache, sleep disturbance
CV: Chest pain, hypertension, peripheral edema
ENDO: Hyperglycemia
EENT: Metallic taste, rhinitis, stomatitis
GI: Abdominal pain, cholecystitis, constipation, diarrhea, esophagitis, flatulence, indigestion, nausea, peptic ulcer, vomiting
GU: Elevated creatinine level
HEME: Leukopenia, thrombocytopenia
MS: Arthralgia, back pain, myalgia
RESP: Cough
SKIN: Alopecia, diaphoresis, dry skin, pruritus, rash, urticaria

Cautions

Administer ursodiol with food to increase drug dissolution.

Give aluminum-containing antacids, cholestyramine, and colestipol at least 1 hour before or 4 hours after ursodiol because they may decrease drug’s effects.

Expect drug to be discontinued if gallstones haven’t partially dissolved after 12 months of therapy.

If patient inadvertently takes too much ursodiol, diarrhea will most likely result and may warrant systemic treatment.

PATIENT SAFTY

Tell patient to take ursodiol with meals.

Urge patient to take aluminum-containing antacids at least 1 hour before or 4 hours after ursodiol to support absorption.

Urge patient to notify prescriber immediately if evidence of acute cholecystitis develops, such as acute right-upper-quadrant abdominal pain.

Inform patient that he may need to take ursodiol for a prolonged period before gallstones dissolve.

Advise diabetic patient to monitor blood glucose levels during therapy because ursodiol may alter blood glucose control.

Category

Chemical class: Human IgG1k monoclonal antibody
Therapeutic class: Antipsoriasitic

Pregnancy category: B

Indications

To treat moderate to severe plaque psoriasis in patients who are candidates for phototherapy or systemic therapy SUBCUTANEOUS INJECTION Adults weighing 100 kg (220 lb) or less: Initial: 45 mg followed by 45 mg 4 wk later and then 45 mg every 12 wk. Adults weighing more than 100 kg (220 lb): Initial: 90 mg followed by 90 mg 4 wk later and then 90 mg ever 12 wk.

Mechanism of Action

Binds to p40 protein subunit used by interleukin (IL)-12 and IL-23 cytokines. These specific cytokines are involved in inflammatory and immune responses, such as natural killer cell activation and CD4+ T-cell differentiation and activation. By disrupting signaling mediated by IL-12 and IL-23, signs and symptoms caused by inflammatory and immune responses in plaque psoriasis are diminished or relieved.

Contraindications

Hypersensitivity to ustekinumab or its components

Interactions

cytochrome P-450 substrates such as cyclosporine, theophylline,
warfarin: Possibly altered effects or blood levels of these when ustekinumab is started or stopped live-virus vaccines: Increased risk of adverse vaccine effects

Side Efect

CNS: Depression, dizziness, fatigue, headache, reversible leukoencephalopathy syndrome
ENDO: Nasopharyngitis, pharyngolaryngeal pain
GI: Diarrhea, diverticulitis, gastroenteritis
GU: UTI
MS: Back pain, myalgia, osteomyelitis
RESP: Pneumonia, upper respiratory tract infection
SKIN: Cellulitis, pruritus
Other: Anti-ustekinumab antibodies, injection site reactions (bruising, erythema, hemorrhage, induration, irritation, pain, pruritus, swelling), malignancies (breast; colon; head and neck; kidney; nonmelanoma of skin, kidney, prostate, thyroid), serious infection including bacterial, fungal and viral infections and reactivation of latent infections

Cautions

Make sure patient has a tuberculin skin test before therapy starts. If skin test is positive, treatment of latent tuberculosis should start before ustekinumab therapy starts. Also expect antituberculosis therapy to start if patient has a history of latent or active tuberculosis but adequate therapy can’t be confirmed or if patient has a negative test for latent tuberculosis but has risk factors for tuberculosis.

Make sure patient is current with all immunizations before starting ustekinumab therapy because patient shouldn’t receive live vaccines during treatment. BCG vaccines shouldn’t be given for 1 year before or after ustekinumab therapy.
WARNING If patient has evidence of an active infection when drug is prescribed, therapy shouldn’t start until infection has been treated. Monitor all patients for infection during therapy, especially those receiving immunosuppressants. If a serious infection, an opportunistic infection, or sepsis develops, expect prescriber to stop ustekinumab and start appropriate antimicrobial therapy.

Patients with a history of cancer or who have genetic deficiencies in IL-12 or IL-23 should be thoroughly evaluated before ustekinumab therapy starts because various cancers have occurred in patients being treated with ustekinumab. Monitor patients throughout therapy for unusual, persistent, or severe signs and symptoms.

Use ustekinumab cautiously in patients with recurrent infection or increased risk of infection and in patients who live in regions where tuberculosis and histoplasmosis are endemic.

Give ustekinumab using a 27G, half-inch needle into upper arms, gluteal region, thighs, or any quadrant of abdomen. Rotate sites, and avoid areas that are tender, bruised, erythematous, or indurated.

Note that needle cover on prefilled syringe contains a latex derivative and shouldn’t be handled by persons with a latex allergy.

Monitor patient for headache, seizures, vision disturbances, and confusion, which may signal reversible posterior leukoencephalopathy syndrome, a rare neurologic disorder that may occur with ustekinumab therapy. If present, notify prescriber, discontinue ustekinumab therapy, and provide appropriate treatment, as ordered.

PATIENT SAFTY

Inform patient that treatment must be supervised by a health care professional.

Inform patient that tuberculosis may occur during ustekinumab therapy. Instruct him to report persistent cough, wasting or weight loss, and low-grade fever to prescriber.

Teach patient to recognize and report evidence of infection; drug may need to be stopped. Advise patient to avoid people with infections and to have all prescribed laboratory tests performed.

Inform patient that the risk of developing certain kinds of cancer is higher in patients taking ustekinumab. Emphasize importance of follow-up visits and reporting any unusual, persistent, or suddenonset signs or symptoms.

Caution against receiving live-virus vaccines while taking ustekinumab; doing so may adversely affect the immune system.

Urge patient to inform all health care providers about ustekinumab use and to inform prescriber about all OTC medications being taken, including herbal remedies and vitamin and mineral supplements.

Category

Chemical class: Carboxylic acid derivative
Therapeutic class: Anticonvulsant

Pregnancy category: D

Indications

To treat simple or complex absence seizures, complex partial seizures, myoclonic seizures, and generalized tonicclonic seizures as monotherapy Adults and adolescents. Initial: 10 to 15 mg/kg/day in divided doses b.i.d. or t.i.d., increased by 5 to 10 mg/kg daily every wk, as needed and as prescribed. Maximum: 60 mg/kg daily. Children. Initial: 15 to 45 mg/kg daily in divided doses b.i.d. or t.i.d., increased by 5 to 10 mg/kg/day every wk, as needed and as prescribed. As adjunct to treat simple or complex absence seizures, complex partial seizures, myoclonic seizures, and generalized tonic-clonic seizures , DELAYED-RELEASE SPRINKLE , DELAYED-RELEASE , SYRUP,
IV: Adults and adolescents.10 to 30 mg/kg/day in divided doses, increased by 5 to 10 mg/ kg/day every wk,as needed and as prescribed. Children.30 to 100 mg/kg daily in divided doses, as prescribed.
DOSAGE ADJUSTMENT For adults being converted from immediate-release divalproex tablets to delayed-release tablets, dosage increased to 8% to 20% more than total daily dose of immediate-release tablets and given once daily. To treat acute manic phase of bipolar disorder
Adults.Initial: 750 mg daily in divided doses. Maximum: 60 mg/kg daily. To prevent migraine headache
Adults.250 mg every 12 hr, increased p.r.n. Maximum: 1 g daily.
Adults.500 mg daily, increased, as needed and prescribed, up to 1 g daily. Maximum: 1 g daily.

Mechanism of Action

May decrease seizure activity by blocking reuptake of gamma-aminobutyric acid (GABA), the most common inhibitory neurotransmitter in the brain. GABA suppresses the rapid firing of neurons by inhibiting voltage-sensitive sodium channels.

Contraindications

Hepatic dysfunction; hypersensitivity to valproic acid, valproate sodium, divalproex sodium, or their components; urea cycle disorders

Interactions

aspirin, heparin, NSAIDs, oral anticoagulants, thrombolytics: Increased inhibition of platelet aggregation and risk of bleeding barbiturates, primidone: Increased blood levels of both , additive CNS effects carbamazepine: Possibly decreased valproic acid effectiveness carbapenem antibiotics (ertapenem, imipenem, meropenem): Reduced serum valproic acid level, causing loss of seizure control cholestyramine: Decreased bioavailability of valproic acid clonazepam: Increased risk of absence seizures
CNS depressants: Increased CNS depression diazepam: Inhibited diazepam metabolism ethosuximide: Unpredictable blood ethosuximide level felbamate: Impaired valproic acid metabolism and increased blood drug level haloperidol, loxapine, MAO inhibitors, maprotiline, phenothiazines, thioxanthenes, tricyclic antidepressants: Increased CNS depression, lowered seizure threshold lamotrigine: Decreased lamotrigine clearance mefloquine: Decreased blood levels of valproic acid, divalproex, and valproate sodium; increased risk of seizures
phenytoin: Increased risk of phenytoin toxicity, loss of seizure control
alcohol use: Additive CNS depression

Side Efect

CNS: Agitation, ataxia, confusion, depression, dizziness, drowsiness, euphoria, hallucinations, headache, hyperesthesia, hypothermia, lack of coordination, lethargy, loss of seizure control, paresthesia, psychosis, sedation, suicidal ideation, tremor, vertigo, weakness
EENT: Diplopia, nystagmus, pharyngitis, spots before eyes
ENDO: Galactorrhea, hyperglycemia
GI: Abdominal pain, anorexia, constipation, diarrhea, elevated liver function test results, hepatotoxicity, increased appetite, indigestion, nausea, pancreatitis, vomiting
GU: Menstrual irregularities
HEME: Eosinophilia, hematoma, leukopenia, prolonged bleeding time, thrombocytopenia
MS: Dysarthria
SKIN: Alopecia, diaphoresis, erythema multiforme, jaundice, petechiae, photosensitivity, pruritus, rash, Stevens-Johnson syndrome
Other: Facial edema, hyperammonemia, injection site pain, weight gain or loss

Cautions

Give oral valproic acid or divalproex with food to minimize GI irritation, if needed.

Administer drug at least 2 hours before or 6 hours after cholestyramine.

Don’t mix syrup with carbonated beverages; result ay be an unpleasant-tasting mixture and irritate mouth and throat.

Don’t break or let patient chew delayedrelease tablets.

As needed, sprinkle contents of delayedrelease sprinkle capsules on small amount of semisolid food just before administration. Instruct patient not to chew contents of delayed-release sprinkle capsules.

For I.V. administration, dilute prescribed dose with at least 50 ml compatible diluent and infuse over 60 minutes.

Patient should be switched from I.V. to P.O. form of valproic acid as soon as possible.

Patient with hypoalbuminemia or another protein-binding deficiency is at increased risk for valproic acid toxicity.

Watch for evidence of decreased hepatic function, including anorexia, facial edema, jaundice, lethargy, loss of seizure control, malaise, vomiting, and weakness.

Monitor liver function test results, as ordered. Assess for signs and symptoms of hepatotoxicity during first 6 months of treatment, especially in children under age 2. Notify prescriber immediately if you suspect hepatotoxicity.

Monitor platelet count, as ordered, for signs of thrombocytopenia, and notify prescriber if they appear.
WARNING Hyperammonemia may occur even if liver function test results are normal. Monitor ammonia levels, as ordered. If patient develops unexplained lethargy, vomiting, or changes in mental status with an increase in ammonia level; if asymptomatic ammonia elevations are detected and persist; or if patient develops hypothermia even without hyperammonemia, expect to discontinue valproic acid.

Watch patient closely for suicidal tendencies, particularly when therapy starts and dosage changes, because depression may worsen temporarily during these times, possibly leading to suicidal ideation.

Monitor patient’s drug level, as ordered, especially early in therapy and if patient takes other because interactions can alter the blood level.

Drug may alter urine ketone test and thyroid function tests.

Category

Chemical class: Nonpeptide tetrazole derivative
Therapeutic class: Antihypertensive

Pregnancy category: C

(first trimester), D (later trimesters)

Indications

To manage hypertension, alone or with other antihypertensives
Adults. Initial: 80 or 160 mg daily, increased as needed and prescribed. Maximum: 320 mg/day. Children ages 6 to 16. 1.3 mg/kg (up to 40 mg total) once daily, increased as needed and prescribed. Maximum: 2.7 mg/kg (up to 160 mg) daily. To treat class II to IV heart failure
Adults.Initial: 40 mg b.i.d., increased to 80 mg b.i.d. and then 160 mg b.i.d., as needed and prescribed. Maximum: 320 mg daily. To reduce cardiovascular mortality in stable patients with left ventricular failure or dysfunction following an MI
Adults. Initial: 20 mg b.i.d. starting as early as 12 hr after MI, increased to 40 mg b.i.d. within 7 days, followed by subsequent adjustments to 160 mg b.i.d., as tolerated. Maintenance: 160 mg b.i.d.
DOSAGE ADJUSTMENT If patient develops symptomatic hypotension or renal dysfunction, dosage decreased.

Mechanism of Action

Blocks the hormone angiotensin II from binding to receptor sites in vascular smooth muscle, adrenal glands, and other tissues. This action inhibits vasoconstrictive and aldosterone-secreting effects of angiotensin II, thereby reducing blood pressure.

Contraindications

Hypersensitivity to valsartan or its components

Interactions

antihypertensives, diuretics: Additive hypotensive effect potassium salts, potassium-sparing diuretics: Possibly hyperkalemia potassium-containing salt substitutes: Possibly hyperkalemia

Side Efect

CNS: Dizziness, fatigue, headache, insomnia
CV: Edema, hypotension, vasculitis
EENT: Pharyngitis, rhinitis, sinusitis
GI: Abdominal pain, diarrhea, elevated liver enzymes, hepatitis, indigestion, nausea, vomiting
GU: Increased blood creatinine level
HEME: Thrombocytopenia
MS: Arthralgia, back pain, rhabdomyolysis
RESP: Cough, upper respiratory tract infection
SKIN: Alopecia, rash
Other: Angioedema, hyperkalemia, viral infection

Cautions

Valsartan shouldn’t be given to patients who have hypovolemia or are taking a diuretic because of increased risk of severe hypotension from volume depletion.

Check patient’s blood pressure often during therapy.

Be aware that maximal blood pressure reduction typically occurs after 4 weeks.

Monitor serum potassium level because drug may elevate potassium level by blocking aldosterone secretion.

PATIENT SAFTY

Instruct patient to take valsartan exactly as prescribed at the same time each day to maintain therapeutic effect.

Advise patient to avoid hazardous activities until drug’s CNS effects are known.

Advise patient to avoid using potassiumcontaining salt substitutes without consulting prescriber.

Instruct female patient of childbearing age to use reliable birth control during therapy and to notify prescriber at once about known or suspected pregnancy because valsartan will need to be discontinued.

Urge patient to keep follow-up appointments to monitor progress.

Category

Chemical class: Tricyclic glycopeptide derivative
Therapeutic class: Antibiotic

Pregnancy category: B

(oral), C (parenteral)

Indications

To treat pseudomembranous colitis caused by Clostridium difficile and enterocolitis caused by staphylococci , Adults and adolescents. 125 to 500 mg every 6 hr for 7 to 10 days. Maximum: 2 g daily. Children. 10 mg/kg (up to 125 mg) every 6 hr for 7 to 10 days. Maximum: 2 g daily. To treat bacterial endocarditis caused by methicillin-resistant Staphylococcus aureus
IV:
Adults. 30 mg/kg daily in equally divided doses b.i.d. for 4 to 6 wk. Maximum: 2 g daily. As adjunct to treat bacterial endocarditis caused by methicillin-resistant S. aureus in patients with prosthetic heart valve
IV:
Adults. 30 mg/kg daily in equally divided doses b.i.d. to q.i.d. for 6 wk or longer in conjunction with rifampin and gentamicin. Maximum: 2 g daily. To treat bacterial endocarditis caused by Streptococcus bovis or Streptococcus viridans
IV:
Adults.30 mg/kg daily in equally divided doses b.i.d. for 4 wk. Maximum: 2 g daily. As adjunct to treat bacterial endocarditis caused by enterococci
IV:
Adults. 30 mg/kg daily in equally divided doses b.i.d. for 4 to 6 wk in conjunction with gentamicin. Maximum: 2 g daily. To treat bacterial septicemia, bone and joint infections, pneumonia, and skin and soft-tissue infections caused by staphylococcus, including methicillinresistant strains, and life-threatening infections
IV: Adults and children age 12 and over. 500 mg every 6 hr or 1 g every 12 hr infused over at least 60 min. Maximum: 4 g daily. Children ages 1 month to 12 years. 10 mg/ kg every 6 hr or 20 mg/kg every 12 hr infused over at least 60 min. Neonates ages 1 week to 1 month.Initial: 15 mg/kg followed by 10 mg/kg every 8 hr infused over at least 60 min. Neonates under age 1 week. Initial: 15 mg/ kg followed by 10 mg/kg every 12 hr infused over at least 60 min.

Mechanism of Action

Inhibits bacterial RNA and cell wall synthesis; alters permeability of bacterial membranes, causing cell wall lysis and cell death.

Incompatibilities

Don’t give I.V. vancomycin through same I.V. line as other . Don’t add to albumin-containing solutions, alkaline solutions, aminophylline, amobarbital sodium, aztreonam, cefepime, ceftazidime, chloramphenicol sodium succinate, chlorothiazide sodium, dexamethasone sodium phosphate, foscarnet sodium, heparin sodium, methicillin sodium, penicillin G, pentobarbital sodium, phenobarbital sodium, piperacillin sodium and tazobactam sodium, secobarbital sodium, and sodium bicarbonate. Vancomycin may precipitate with heavy metals.

Contraindications

Hypersensitivity to vancomycin or its components, hypersensitivity to corn or corn products when vancomycin is given with dextrose solutions

Interactions

aminoglycosides (amikacin, gentamicin, tobramycin), amphotericin B, bacitracin (parenteral), bumetanide, capreomycin, carmustine, cidofovir, cisplatin, cyclosporine, ethacrynic acid, furosemide, paromomycin, pentamidine (parenteral), polymyxins, salicylates (parenteral), streptozocin: Additive nephrotoxicity or ototoxicity antihistamines, buclizine, cyclizine, meclizine, phenothiazines, thioxanthenes, trimethobenzamide: Masked symptoms of ototoxicity cholestyramine, colestipol: Decreased antibacterial activity of oral vancomycin dexamethasone: Decreased penetration of vancomycin into CSF nephrotoxic : Increased risk of nephrotoxicity

Side Efect

CNS: Chills, dizziness, vertigo
CV: Hypotension
EENT: Ototoxicity
GI: Nausea, pseudomembranous colitis
GU: Nephrotoxicity
HEME: Eosinophilia, neutropenia
RESP: Dyspnea, wheezing
SKIN: Exfoliative dermatitis; drug rash with eosinophilia and systemic symptoms (DRESS); extravasation with pain, tenderness, thrombophlebitis, and tissue necrosis; pruritus; rash; toxic epidermal necrolysis; urticaria
Other: Anaphylaxis, drug-induced fever, injection site inflammation, superinfection

Cautions

To reconstitute 500-mg vial of vancomycin for I.V. use, add 10 ml of sterile water for injection; further dilute with at least 100 ml of compatible I.V. solution. For 1-g vial of dry, sterile powder, add 20 ml of sterile water for injection; further dilute with at least 200 ml of compatible I.V. solution.
WARNING Infuse over at least 1 hour. Rapid delivery may cause hypotension or transient “red man syndrome,”characterized by chills; fainting; fever; flushing of face, neck, upper arms, and torso; hypotension; nausea; tachycardia; and vomiting.

Monitor blood vancomycin levels, as ordered; therapeutic levels are 10 to 15 mcg/ ml trough and 30 to 40 mcg/ml peak.

Monitor serum vancomycin concentration in patients with renal impairment or colitis because significant increases in blood drug level have occurred in such patients taking multiple oral doses of vancomycin.

If patient has an inflammatory intestinal disorder, assess him often for adverse reactions because vancomycin absorption may be increased in these conditions.

Check CBC results and serum creatinine and BUN levels during therapy, especially if patient has renal impairment or takes an aminoglycoside.

Observe I.V. infusion site for evidence of extravasation, including necrosis, pain, tenderness, and thrombophlebitis. If extravasation occurs, discontinue infusion immediately and notify prescriber.

Assess hearing during therapy. Transient or permanent ototoxicity may occur if patient receives an excessive amount of drug, has an underlying hearing loss, or receives concurrent aminoglycosides.

Monitor patient closely for diarrhea because it may indicate pseudomembranous colitis aused by Clostridium difficile, a risk with many antibiotics. If diarrhea occurs during therapy, notify prescriber and expect to withhold drug. If confirmed, treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

PATIENT SAFTY

Instruct patient to use a calibrated measuring device to accurately measure doses of oral solution.

Advise patient to notify prescriber if no improvement occurs after a few days.

Instruct patient to complete full course of vancomycin, as prescribed.

Instruct patient to notify prescriber if she develops severe or persistent diarrhea.

Instruct patient to keep follow-up appointments during and after treatment.

Category

Chemical class: Phosphodiesterase type 5 inhibitor
Therapeutic class: Anti-impotence agent

Pregnancy category: B

Indications

To treat erectile dysfunction
Adults. 10 mg taken 1 hr before sexual activity; increased to 20 mg or decreased to 5 mg, as needed. Maximum: 20 mg and once-daily limit regardless of dosage.
DOSAGE ADJUSTMENT If patient takes ritonavir, vardenfil dosage shouldn’t exceed 2.5 mg in 72 hr. If patient takes indinavir, saquinavir, atazanavir, clarithromycin, ketoconazole 400 mg daily, itraconazole 400 mg daily, or another potent CYP3A4 inhibitor, vardenafil dosage shouldn’t exceed 2.5 mg in 24 hr. If patient takes ketoconazole 200 mg and itraconazole 200 mg daily, vardenafil dosage shouldn’t exceed 5 mg in 24 hr.

Mechanism of Action

Enhances effect of nitric oxide (released in the penis by sexual stimulation) and inhibits phosphodiesterase type 5, which increases cGMP level, relaxes smooth muscle, and increases blood flow into the corpus cavernosum, producing an erection.

Contraindications

Concurrent administration of alpha blockers, concurrent continuous or intermittent nitrate therapy, hypersensitivity to vardenafil or its components

Interactions

alpha blockers, nitrates: Profound hypotension atazanavir, clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, ritonavir, saquinavir: Increased vardenafil effects class IA (procainamide, quinidine) and class III (amiodarone, sotalol) antiarrhythmics: Possibly increased QT-interval prolongation indinavir, ritonavir: Reduced blood levels of indinavir and ritonavir grapefruit juice: Possibly increased vardenafil effect

Side Efect

CNS: Dizziness, headache, seizures, transient global amnesia
CV: Hypotension
EENT: Decreased vision, hearing loss, nonarteritic anterior ischemic optic neuropathy, rhinitis, sinusitis, tinnitus
GI: Indigestion, nausea
MS: Back pain
SKIN: Flushing
Other: Flulike symptoms, increased creatine kinase level

Cautions

Vardenafil shouldn’t be used by men taking class IA (procainamide, quinidine) or class III (amiodarone, sotalol) antiarrhythmics or by men who have congenital prolonged QT interval. Drug may potentiate prolonged QT interval.

Use vardenafil cautiously in men with renal or hepatic dysfunction, in elderly men, and in men with penile abnormalities that may predispose them to priapism.

Also use cautiously in patients with left ventricular outflow obstruction, such as aortic stenosis, and those with severely impaired autonomic control of blood pressure. These conditions increase sensitivity to vasodilators, such as vardenafil.

Monitor blood pressure and heart rate before and after giving drug, especially if patient takes an alpha blocker, because of increased risk of symptomatic hypotension.

Monitor patient’s vision, especially if he’s over age 50; has diabetes, hypertension, coronary artery disease, or hyperlipidemia; or smokes, because vardenafil rarely leads to nonarteritic ischemic optic neuropathy and decreased vision, possibly permanent.

Monitor patient’s hearing. Sudden decrease or loss, possibly with tinnitus and dizziness, may occur with vardenafil use. Report such changes immediately, and expect drug to be discontinued.

PATIENT SAFTY

For best results, tell patient to take drug 1 hour before anticipated sexual activity.
WARNING Tell patient not to take vardenafil if he takes an organic nitrate, continuously or intermittently, or within 4 hours of taking an alpha blocker because profound hypotension and death could result.

Caution patient not to take vardenafil more than once daily or to exceed 20 mg daily.

Tell patient to stop taking vardenafil and notify prescriber if he has a sudden loss of vision in one or both eyes, sudden hearing loss, seizures, or trouble remembering.

Advise patient to seek sexual counseling to enhance drug’s effects.

To avoid possible penile damage and permanent loss of erectile function, urge patient to notify prescriber at once if erection is painful or lasts longer than 4 hours.

Category

Chemical class: Tartrate salt
Therapeutic class: Nicotinic blocker Pregnancy classification: C

Indications

As adjunct to smoking cessation treatment
Adults. Initial: 0.5 mg daily for 3 days; then increased to 0.5 mg b.i.d. for 4 days, and then increased to 1 mg b.i.d. for a total of 12 wk of therapy. If effective, an additional 12 wk of therapy may be given.
DOSAGE ADJUSTMENT If patient has severe renal impairment, maximum dosage is 0.5 mg b.i.d. If patient is having hemodialysis for end-stage renal disease, maximum dosage is 0.5 mg daily.

Mechanism of Action

Blocks nicotine from activating alpha4beta2 receptors by binding to them. This inhibits nicotine stimulation of the central nervous mesolimbic dopamine system, which probably is the area that produces pleasure in and reinforcement of smoking.

Contraindications

Hypersensitivity to varenicline or its components

Interactions

nicotine (transdermal): Increased adverse reactions

Side Efect

CNS: Abnormal dreams, agitation, anxiety, asthenia, attention difficulties, behavior changes, delusions, depression, dizziness, dysgeusia, fatigue, hallucinations, headache, homicidal ideation, hostility, insomnia, irritability, lethargy, loss of consciousness, malaise, mania, mental impairment, panic, paranoia, psychosis, restlessness, sensory disturbances, seizures, somnolence, stroke, suicidal ideation, thirst
CV: Angina, chest pain, edema, hypertension, MI, peripheral ischemia, thrombosis, ventricular extrasystoles
EENT: Dry mouth, epistaxis, gingivitis, rhinorrhea
ENDO: Hot flashes
GI: Abdominal pain, acute pancreatitis, anorexia, constipation, diarrhea, dyspepsia, flatuence, gastroesophageal reflux disease, GI hemorrhage, increased appetite, liver enzyme abnormalities, nausea, vomiting
GU: Acute renal failure, polyuria, urine retention
HEME: Leukocytosis, lymphadenopathy, splenomegaly, thrombocytopenia
RESP: Asthma, dyspnea, pulmonary embolism
MS: Arthralgia, back pain, muscle cramp, musculoskeletal pain, myalgia
SKIN: Diaphoresis, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome, urticaria
Other: Angioedema, flulike syndrome, hyperkalemia, hypersensitivity, hypokalemia

Cautions

Use cautiously in patients with renal disease because varenicline is substantially excreted by the kidneys.

Review patient’s medication history before starting varenicline because dosage adjustments may be needed for such as theophylline, warfarin, and insulin.
WARNING Monitor patient for angioedema, difficult breathing, rash with mucosal lesions, or other signs of hypersenstivity. Report immediately, stop varenicline therapy, and provide supportive emergency care, as prescribed.

If patient has nausea, the most common adverse reaction to varenicline, notify prescriber. Dosage reduction may help.

Even with varenicline therapy, nicotine withdrawal symptoms and worsening of underlying psychiatric illness may occur with smoking cessation. Monitor patient for neurospychiatric symptoms, including changes in behavior, hostility, agitation, depressed mood, suicidal ideation, and worsening of pre-existing psychiatric illness. If present, notify prescriber immediately, institute safety measures, and expect drug to be discontinued.

Watch patient closely for suicidal tendencies, particularly when therapy starts and dosage changes, because depression may worsen temporarily during these times, possibly leading to suicidal ideation.

PATIENT SAFTY

Explain that using nicotine patches while taking varenicline won’t increase its effectiveness and may increase

Side Efect

such as dizziness, nausea, and vomiting.

Instruct patient to set a date to quit smoking and then start taking varenicline 1 week before the quit date.

Explain how to adjust dose when drug is used for smoking cessation. Tell patient to take drug after eating and with a full glass of water.

Encourage patient to continue trying to stop smoking even if an early relapse occurs during varenicline therapy.
WARNING Tell patient to seek medical attention immediately if he develops swelling of his face, mouth, limbs, or neck; difficulty breathing; mucosal lesions; or any other signs of hypersensitivity during therapy.

Inform patient that the most common

Side Efect

to varenicline therapy are nausea and insomnia, usually transient. If they persist, patient should notify prescriber; dosage reduction may help.

Caution patient to avoid hazardous activities until CNS effects of drug are known. Explain that near miss traffic accidents and other accidential injuries have occurred in patients taking varenicline.

Explain that vivid, unusual, or strange dreams may occur during therapy.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes.

Tell patient that nicotine withdrawal can occur even with varenicline use and that pre-existing mental illness may worsen during smoking cessation. Advise patient or family to notify prescriber about abnormal thinking or behavior and to stop taking drug immediately.

Category

Chemical class: Polypeptide hormone
Therapeutic class: Antidiuretic

Pregnancy category: C

Indications

To prevent or control symptoms of central diabetes insipidus caused by insufficient ADH I.M.OR SUBCUTANEOUS INJECTION
Adults.5 to 10 units b.i.d. or t.i.d., as needed. Children.2.5 to 10 units t.i.d. or q.i.d., as needed. To prevent or treat abdominal distention
I.M.INJECTION
Adults.5 units, increased to 10 units every 3 to 4 hr, as needed.

Contraindications

Chronic nephritis with nitrogen retention, hypersensitivity to vasopressin or its components

Interactions

carbamazepine, chlorpropamide, clofibrate, fludrocortisone, tricyclic antidepressants: Increased antidiuretic effect demeclocycline, lithium, norepinephrine: Decreased antidiuretic effect

Side Efect

CNS: Dizziness, headache, light-headedness, tremor
CV: Angina, MI
EENT: Circumoral pallor
ENDO: Water intoxication
GI: Abdominal cramps, diarrhea, eructation, flatulence, intestinal hypermotility, nausea, vomiting
SKIN: Diaphoresis, pallor
Other: Allergic reaction Vasopressin

Mechanism of Action

Vasopressin, a synthetic form of antidiuretic hormone, treats diabetes insipidus by decreasing urine output and raising urine osmolality.When vasopressin attaches to vasopressin2 (V2) receptors on cell membranes in the nephron’s collecting duct, it activates the enzyme adenyl cyclase to convert adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP). This action increases the collecting duct’s permeability and enhances water reabsorption into the blood.

Cautions

Use vasopressin with extreme caution in patients with coronary artery disease because it may cause angina or MI; in those with hypertension because it may increase blood pressure; and in those with asthma, epilepsy, heart failure, or migraine headache because extracellular fluid may increase rapidly.

Monitor fluid and electrolyte balance during therapy. Check intake and output at least every 8 hours, and watch for evidence of water intoxication and hyponatremia, including anuria, confusion, drowsiness, headache, listlessness, and weight gain.

PATIENT SAFTY

Teach patient how to administer vasopressin; stress the need to rotate injection sites.

Urge patient to notify prescriber immediately if he has evidence of possible water intoxication, including anuria, confusion, drowsiness, headache, listlessness, and unexplained weight gain.

Inform patient that abdominal cramps, nausea, and skin blanching will subside after a few minutes and can be minimized by drinking one or two glasses of water.

Category

Chemical class: Phenylethylamine derivative
Therapeutic class: Antidepressant

Pregnancy category: C

Indications

To treat and prevent relapse of major depression
Adults.75 mg daily with a meal at same time each day, morning or evening (for some patients, 37.5 mg daily for 4 to 7 days before increasing to 75 mg daily); then increased by 75 mg daily every 4 days, as prescribed. Maximum: 225 mg daily.
DOSAGE ADJUSTMENT Initial daily dose decreased by 25% to 50% for patients with mild to moderate renal impairment and by 50% for patients with hepatic impairment.
Adults. 50 mg daily, with a meal, at the same time each day morning or evening
DOSAGE ADJUSTMENT For patients with severe renal impairment and for elderly patients having difficulty tolerating drug, 50 mg every other day.
Adults. 75 mg daily in divided doses b.i.d. or t.i.d., increased by 75 mg daily every 4 days, as prescribed. Maximum: 375 mg daily (225 mg/day for outpatients). To treat generalized anxiety disorder or social anxiety disorder (EFFEXOR XR)
Adults.75 mg daily with a meal at same time each day, morning or evening (for some patients, 37.5 mg daily for 4 to 7 days before increasing to 75 mg daily); then increased by 75 mg daily every 4 days, as prescribed. Maximum: 225 mg daily.
DOSAGE ADJUSTMENT Initial daily dose decreased by 25% to 50% for patients with mild to moderate renal impairment and by 50% for patients with hepatic impairment.

Mechanism of Action

Inhibits neuronal reuptake of serotonin and norepinephrine, along with its active metabolite, O-desmethylvenlafaxine. These actions raise serotonin and norepinephrine levels at nerve synapses, elevating mood and reducing depression.

Contraindications

Hypersensitivity to desvenlafaxine, venlafaxine, or their components; use of an MAO inhibitor within 14 days

Interactions

amitriptyline, clomipramine, desipramine, doxepin, haloperidol, imipramine, linezolid, lithium, nortriptyline, protriptyline, St. John’s wort, tramadol, trazodone, triptans: Possibly serotonin syndrome aspirin, NSAIDs,
warfarin: Increased risk of bleeding venlafaxine hydrochloride 1082
cimetidine: Decreased clearance and increased levels of desvenlafaxine and venlafaxine clozapine: Possibly increased blood clozapine level and serious

Side Efect

, including seizures CYP3A4 inhibitors,
ketoconazole: Increased plasma venlafaxine level and risk of adverse reactions
MAO inhibitors: Increased risk of hypertension; hyperthermia; mental status changes, including coma and delirium; muscle rigidity; and severe myoclonus metoprolol: Increased plasma metoprolol level but decreased effectiveness in lowering blood pressure
warfarin: Possibly increased PT, partial thromboplastin time, and INR

Side Efect

CNS: Abnormal dreams, agitation, amnesia, anxiety, asthenia, cerebral ischemia, chills, confusion, delusions, depersonalization, depression, dizziness, dream disturbances, drowsiness, dyskinesia, fever, headache, hyp-esthesia, hypomania, impaired balance and coordination, insomnia, mania, migraine, mood changes, nervousness, neuroleptic malignant syndrome, paresthesia, seizures, serotonin syndrome, somnolence, suicidal ideation, syncope, tremor, vertigo
CV: Arrhythmias, AV block, chest pain, congestive heart failure, elevated cholesterol and triglyceride levels, edema, extrasystoles, hypertension, hypotension, MI, palpitations, sinus tachycardia, thrombophlebitis, vasodilation, worsening of peripheral vascular disease
EENT: Abnormal vision, accommodation abnormality, angle-closure glaucoma, blurred vision, dry mouth, mydriasis, pharyngitis, rhinitis, taste alteration, tinnitus
ENDO: Hyperglycemia, syndrome of inappropriate ADH secretion
GI: Abdominal pain, anorexia, colitis, constipation, diarrhea, elevated liver enzymes, flatulence, GI hemorrhage, indigestion, nausea, vomiting
GU: Anorgasmia (women), decreased libido, ejaculation disorder, impotence, urinary incontinence or urgency, urine retention
HEME: Anemia, leukocytosis, leukopenia, lymphadenopathy, thrombocytopenia
MS: Neck pain, rhabdomyolysis
RESP: Cough, eosinophilic pneumonia, increased dyspnea, interstitial lung disease
SKIN: Diaphoresis, ecchymosis, pruritus, Stevens-Johnson syndrome, toxic epidermal necrolysis
Other: Angioedema, hyponatremia, weight loss

Cautions

Use cautiously in patients with a history of mania because desvenlafaxine and venlafaxine therapy may worsen condition. Also use cautiously in patients with a history of seizures, and expect to discontinue drug, as ordered, if seizures occur.

Use cautiously in patients who have medical conditions that might be made worse by an increased heart rate, as in hyperthyroidism, heart failure, or recent MI.
WARNING Be aware that serotonin syndrome in its most severe form may resemble neuroleptic malignant syndrome, which includes hyperthermia, muscle rigidity, autonomic instability with possibly rapid changes in vital signs, and mental status changes. Stop drug immediately and provide supportive care.

Monitor blood pressure often during therapy because it may cause dose-related sustained increase in supine diastolic pressure. Expect to reduce or stop drug, as prescribed, if increase develops.

Assess patient’s electrolyte balance, as ordered, because drug can cause hyponatremia, especially in elderly patients and in patients who take diuretics or are volumedepleted. If patient has evidence of hyponatremia (headache, trouble concentrating, confusion, weakness, unsteadiness), notify prescriber. If imbalance is confirmed, expect to stop drug and give appropriate care.

Watch patient for suicidal tendencies, especially when therapy starts and dosage changes.
WARNING Drug shouldn’t be stopped abruptly because doing so may cause multiple adverse effects, including asthenia, dizziness, headache, insomnia, nervousness, and flulike symptoms.

PATIENT SAFTY

Instruct patient not to crush or chew capsules or tablets. If she has trouble swallowing capsules, tell her to open capsule, sprinkle contents on a spoonful of applesauce, and swallow immediately without chewing, followed by a glass of water.

Advise patient to avoid alcohol during venlafaxine therapy.

Advise patient not to stop taking desvenlafaxine or venlafaxine abruptly.

Caution patient to notify prescriber if she becomes pregnant during therapy because she’ll need a different antidepressant. Taking desvenlafaxine or venlafaxine during third trimester of pregnancy increases risk of complications in the newborn.

Advise patient to tell prescriber about all other prescribed or OTC products she takes because of risk of interactions.

Urge caregivers to monitor patient closely for suicidal tendencies, especially when therapy starts or dosage changes.

Caution patient to avoid aspirin and NSAIDs, if possible, while taking desvenlafaxine or venlafaxine.

Category

Chemical class: Phenylalkylamine derivative
Therapeutic class: Antianginal, antiarrhythmic, antihypertensive

Pregnancy category: C

Indications

To treat chronic angina pectoris Adults and adolescents age 15 and over. Initial: 80 to 120 mg t.i.d., increased every day or wk, as needed and prescribed. Maximum: 480 mg daily in divided doses. Infants and children up to age 15. 4 to 8 mg/kg daily in divided doses. To manage hypertension Adults and adolescents age 15 and over. Initial: 80 to 120 mg t.i.d., increased every day or wk, as needed and prescribed. Maximum: 480 mg daily in divided doses.
DOSAGE ADJUSTMENT Initial P.O. dosage possibly reduced to 40 mg t.i.d. (120 mg daily for tablets or capsules) for elderly patients and those with impaired hepatic or left ventricular function. Adults and adolescents age 15 and over. Initial: 5 to 10 mg slowly over 2 min; then 10 mg, as prescribed, if response isn’t adequate after 30 min. Children ages 1 to 15. Initial: 100 to 300 mcg/kg slowly over 2 min, up to maximum of 5 mg; then 10 mg, as prescribed, if response isn’t adequate after 30 min. Infants up to age 1. Initial: 100 to 200 mcg/ kg slowly over 2 min.
DOSAGE ADJUSTMENT I.V. drug administered over 3 minutes in elderly patients.

Mechanism of Action

Inhibits calcium movement into coronary and vascular smooth-muscle cells by blocking slow calcium channels in cell membranes. The resulting decrease in intracellular calcium level has the following effects:

inhibits smooth-muscle cell contractions

decreases myocardial oxygen demand by relaxing coronary and vascular smooth muscle, reducing peripheral vascular resistance, and decreasing systolic and diastolic pressures

slows AV conduction time and prolongs AV nodal refractoriness

interrupts reentry circuit in AV nodal reentrant tachycardias.

Incompatibilities

Don’t mix I.V. verapamil with albumin, amphotericin B injection, hydralazine hydrochloride injection, nafcillin, or sulfamethoxazole and trimethoprim injection. Solutions with pH above 6.0 cause precipitation.

Contraindications

Cardiogenic shock, concomitant use of beta blockers (with I.V. verapamil), hypersensitivity to verapamil or its components, hypotension, severe heart failure unless secondary to supraventricular tachycardia that responds to verapamil, severe left ventricular dysfunction, sick sinus syndrome or secondor third-degree heart block unless artificial pacemaker is in place, ventricular tachycardia (with I.V. verapamil)

Interactions

alpha blockers, antihypertensives, general anesthetics (hydrocarbon), prazosin: Hypotensive effects aspirin: Increased bleeding time
beta blockers: Increased risk of heart failure, hypotension, and severe bradycardia calcium supplements: Decreased response to verapamil carbamazepine, cyclosporine, theophylline, valproate: Increased risk of toxicity from these
cimetidine: Decreased metabolism and increased blood level of verapamil
clonidine: Increased risk of severe sinus bradycardia cyclophosphamide, oncovin, procarbazine, prednissone (COPP) regimen; vindesine, adriamycin, cisplatin (VAC) regimen: Decreased verapamil absorption dantrolene: Increased risk of hyperkalemia and myocardial depression digoxin: Increased blood digoxin level and risk of digitalis toxicity disopyramide, flecainide: Additive negative inotropic effects doxorubicin: Increase plasma doxorubicin level erythromycin, ritonavir: Increased blood verapamil level lithium: Increased risk of neurotoxicity neuromuscular blockers: Prolonged recovery from neuromuscular blockade NSAIDs, sympathomimetics: Decreased antihypertensive effect of verapamil paclitaxel: Decreased paclitaxel clearance phenobarbital: Increased verapamil clearance procainamide: Increased QT interval, additive negative inotropic effects protein-bound (hydantoins, salicylates, sulfonamides, sulfonylureas, and warfarin and other oral anticoagulants): Altered blood levels of these
quinidine: Increased risk of quinidine toxicity, increased QT interval, additive negative inotropic effects
rifampin: Decreased bioavailability of oral verapamil telithromycin: Increased risk of bradyarrhythmias, hypotension, and lactic acidosis grapefruit juice: Increased verapamil level
alcohol use: Increased blood alcohol level and prolonged CNS effects

Side Efect

CNS: Asthenia, confusion, disequilibrium, dizziness, equilibrium disorders, extrapyramidal reactions, fatigue, headache, insomnia, paresthesia, psychosis, shakiness, somnolence, stroke, syncope
CV: Abnormal ECG, angina, AV conduction disorders, bradycardia, claudication, heart failure, hypertension, hypotension, MI, palpitations, peripheral edema, tachycardia, vasculitis
EENT: Blurred vision, dry mouth, tinnitus
ENDO: Gynecomastia, hyperprolactinemia
GI: Constipation, diarrhea, elevated liver function test results, GI distress, nausea
GU: Galactorrhea, impotence, increased urination, menstrual irregularities
MS: Arthralgia, muscle spasms
RESP: Dyspnea, pulmonary edema,
SKIN: Alopecia, diaphroesis, ecchymosis, erythema multiforme, exanthema, flushing, hyperkeratosis, rash, Stevens-Johnson syndrome, urticaria
Other: Allergy aggravated

Cautions

Administer I.V. verapamil with compatible solutions, including Ringer’s injection, D5W, or normal saline solution.

Maintain continuous ECG monitoring and keep emergency resuscitative equipment and readily available during I.V. therapy.

Assess patient with hypertrophic cardiomyopathy or idiopathic hypertrophic subaortic stenosis for early development of hypotension and pulmonary edema because second-degree AV block and sinus arrest can result.

Assess for bradycardia and hypotension, and notify prescriber if heart rate or blood pressure declines significantly.

Disopyramide or flecainide shouldn’t be given within 48 hours before or 24 hours after verapamil because additive negative inotropic effects can result.

Institute measures to prevent constipation, including a high-fiber diet and a stool softener, as prescribed.

PATIENT SAFTY

Instruct patient not to crush or chew verapamil tablets or capsules. Inform her that she may break tablets in half if necessary to aid swallowing.

Direct patient to check her pulse before taking verapamil and to notify prescriber if it’s below 50 beats/minute or as instructed by prescriber.

Caution patient about possible dizziness and the need to avoid potentially hazardous activities until drug’s CNS effects are known.

Inform patient that adverse skin reactions may subside with continued verapamil use. Advise her to notify prescriber if rash persists.

Encourage patient to increase dietary fiber intake to help prevent constipation. Advise her to notify prescriber if problem becomes persistent or severe.

Category

Chemical class: Amino-hexenoic acid Therapeutic: class Anticonvulsant

Pregnancy category: C

Indications

As adjunct therapy for refractory complex partial seizures in patients with inadequate response to several alternative treatments and for whom potential benefits outweigh the risk of vision loss
Adults. Initial: 500 mg twice daily, increased weekly in 500 mg increments, as needed. Maximum: 1.5 g twice daily.
DOSAGE ADJUSTMENT For patient with mild renal impairment (creatinine clearance 51 to 80 ml/min/1.73 m2), reduce dose by 25%. For patients with moderate renal impairment (creatinine clearance 31 to 50 ml/min/1.73 m2), reduce dose by 50%. For patients with severe renal impairment (creatinine clearance 11 to 30 ml/min/ 1.73 m2), reduce dose by 75%. As monotherapy for pediatric patients with infantile spasms for whom potential benefits outweight risk of vision loss

ORALL

Children age 1 month to 2 years.Initial: 50 mg/kg/day in 2 divided doses, increased every 3 days by 25 to 50 mg/kg/day, as needed. Maximum: 150 mg/kg/day.
DOSAGE ADJUSTMENT For patient with mild renal impairment (creatinine clearance 51 to 80 ml/min), reduce dose by 25%. For patients with moderate renal impairment (creatinine clearance 31 to 50 ml/min/ 1.73 m2), reduce dose by 50%. For patients with severe renal impairment (creatinine clearance 11 to 30 ml/min/1.73 m2), reduce dose by 75%.

Mechanism of Action

Inhibits the action of gamma aminobutyric acid transaminase (GABA-T), the enzyme responsible for metabolism of the inhibitory neurotransmitter GABA. This increases GABA level in the CNS, which may play a role in suppression of seizure activity.

Contraindications

Hypersensitivity to vigabatrin and its components

Interactions

phenytoin: Decreased serum phenytoin level

Side Efect

CNS: Abnormal magnetic resonance imaging (MRI), abnormal behavior or dreams, acute psychosis, anxiety, apathy, asthenia, attention disturbance, confusion, coordination abnormality, delirium, depression, dizziness, encephalopathy, expressive language disorder, fatigue, fever, gait disturbance, headache, hyperreflexia, hypertonia, hypoaesthesia, hyporeflexia, hypomania, hypotonia, insomnia, irritability, lethargy, malaise, malignant hyperthermia, memory loss, myoclonus, nervousness, paraesthesia, peripheral neuropathy, postictal state, seizures, sensory disturbance, somnolence, status epilepticus, suicidal ideation, thirst, tremor, vertigo
CV: Chest pain, edema, peripheral edema
EENT: Asthenopia, blurred vision, deafness, diplopia, eye pain, laryngeal edema, nasopharyngitis, nsytagmus, optic neuritis, pharyngolaryngeal pain, tinnitus, toothache, vision loss (severe), visual field defect
GI: Abdominal or stomach pain, cholestasis, constipation, decreased liver enzymes, diarrhea, distention, dyspepsia, esophagitis, GI hemorrhage, nausea, vomiting
GU: Dysmenorrhea, erectile dysfunction, UTI
HEME: Anemia
MS: Arthralgia; back or limb pain; dysarthria; muscle spasticity, spasms or twitching
RESP: Bronchitis, cough, pulmonary edema, respiratory failure, stridor, upper respiratory infection
SKIN: Facial edema, maculopapular rash, pruritus,
Other: Angioedema, birth defects, developmental delay, influenza, multi-organ failure, weight gain

Cautions

Vigabatrin therapy is only available under a restricted distribution program called the SHARE program (1-888-45-SHARE).
WARNING Monitor patient’s vision, and make sure patient has been examined by an ophthalmic professional in which visual fields and retinal examination has been performed no later than 4 weeks after vigabatrin therapy has begun and then periodically thereafter because drug can cause progressive and permanent bilateral concentric visual field constriction and reduce visual acuity. Be aware that while risk increases with total dose and duration of therapy, all patients are at risk for visual abnormalities even after drug has been stopped. Because of the risk of permanent and possibly severe vision loss, drug can be prescribed and obtained only through the SHARE distribution program. Report any visual abnormalities immediately, and expect drug to be discontinued.

Abnormal MRI results have been noted in some infants receiving vigabatrin.

Monitor patient for suicidal ideation throughout therapy but especially when therapy starts or dosage changes.

When discontinuing vigabatrin therapy, expect to do so gradually by decreasing daily dose by 1 gram each week until drug is discontinued, as ordered.

When discontinuing vigabatrin therapy in children, expect to do so gradually by decreasing dose by 25 to 50 mg/kg/day every 3 to 4 days.

Monitor patient for evidence of peripheral neuropathy, such as numbness or tingling in toes or feet, reduced distal lower limb vibration or position sense, or progressive loss of reflexes, starting at the ankles. Alert prescriber if abnormalities are present.

Assess patient routinely for edema, including peripheral edema.

PATIENT SAFTY

Explain the risk of possibly permanent vision loss before patient starts vigabatrin.

Warn patient not to stop taking vigabatrin abruptly; it will need to be weaned off gradually over several weeks.

Advise female patient of childbearing age to use effective contraception if sexually active and to report suspected or confirmed pregnancy immediately.

Advise patient or caregiver to notify prescriber if patient has unusual feelings or behaviors, especially if related to suicidal ideation and particularly at the beginning of therapy and during
DOSAGE ADJUSTMENTs.

Caution patient not to perform hazardous activities such as operating equipment until CNS effects of the drug are known.

Alert patient to monitor his weight because drug may cause weight gain.

Category

Chemical class: Triazole
Therapeutic class: Antifungal

Pregnancy category: D

Indications

To treat invasive aspergillosis; to treat serious fungal infections caused by Scedosporium apiospermum and Fusarium species, including Fusarium solani, in patients intolerant of or refractory to other therapy
IV: Adults and children age 12 and over. Initial: 6 mg/kg over 1 to 2 hr at no more than 3 mg/kg/hr every 12 hr for 2 doses. Maintenance: 4 mg/kg over 1 to 2 hr at no more than 3 mg/kg/hr every 12 hr. Adults and children age 12 and over weighing 40 kg (88 lb) or more. Maintenance: 200 mg every 12 hr, increased to 300 mg every 12 hr, as needed, and taken at least 1 hr before or after a meal. Adults and children age 12 and over weighing less than 40 kg. Maintenance: 100 mg every 12 hr, increased to 150 mg every 12 hr, as needed, and taken at least 1 hr before or after a meal. To treat candidemia in nonneutropenic patients and other deep-tissue disseminatinated Candida infections involving the abdomen, kidney, bladder wall, skin, or a wound
IV:
Adults.Initial: 6 mg/kg over 1 to 2 hr at no more than 3 mg/kg/hr every 12 hr for 2 doses. Maintenance: 3 to 4 mg/kg over 1 to 2 hr at no more than 3 mg/kg/hr every 12 hr for at least 14 days after symptoms resolve or last positive culture, whichever takes longer.
Adults. Maintenance: 200 mg every 12 hr taken at least 1 hr before or after a meal. To treat esophageal candidiasis
Adults. 200 mg every 12 hr taken at least 1 hr before or after a meal for at least 14 days and at least 7 days after signs and symptoms resolve.
DOSAGE ADJUSTMENT If patient can’t tolerate drug, I.V. maintenance dose may be reduced to 3 mg/kg every 12 hr and oral maintenance dose by 50-mg decrements to at least 200 mg every 12 hr (100 mg every 12 hr for patients weighing less than 40 kg). For use with phenytoin, maintenance dose may be increased to 5 mg/kg I.V. every 12 hr or from 200 mg to 400 mg P.O. every 12 hr (100 mg to 200 mg every 12 hr for patients weighing less than 40 kg). For patients with mild to moderate hepatic cirrhosis, standard loading dose should be used but maintenance dose halved for I.V. or P.O. use. For patients with moderate to severe renal insufficiency (creatinine clearance greater than 50 ml/min/1.73 m2), only the oral form should be given, if possible.

Mechanism of Action

Prevents fungal ergosterol biosynthesis by inhibiting fungal cytochrome P-450–mediated 14 alpha-lanosterol demethylation. The loss of ergosterol in the fungal cell wall renders the fungal cell inactive.

Incompatibilities

Don’t infuse into the same line or cannula with other , including parenteral nutrition, to prevent an increase in subvisible particulate matter. Avoid infusion with blood products and any electrolyte supplements. Don’t dilute with 4.2% sodium bicarbonate infusion because the mildly alkaline nature of the diluent causes slight degradation of voriconazole after 24 hours of storage at room temperature.

Contraindications

Coadministration with long-acting barbiturates, carbamazepine, CYP3A4 substrates (astemizole, cisapride, pimozide, quinidine, or terfenadine), efavirenz, ergot alkaloids, rifabutin, rifampin, ritonavir, sirolimus, or St. John’s wort; hypersensitivity to voriconazole or its components; galactose intolerance, glucose-galactose malabsorption, or Lapp lactase deficiency (oral form only contains lactose)

Interactions

alfentanil: Increased plasma alfentanil level and increased risk of

Side Efect

benzodiazepines: Possibly prolonged sedative effect of benzodiazepines calcium channel blockers; HMG-CoA reductase inhibitors, such as lovastatin; omeprazole; sirolimus: Possibly increased plasma levels of these , leading to increased risk of

Side Efect

and toxicity carbamazepine, long-acting barbiturates, phenytoin,
rifampin: Decreased plasma voriconazole concentration coumarin,
warfarin: Possibly increased PTT cyclosporine, sirolimus, tacrolimus: Increased serum concentrations of these and risk of toxicity, especially nephrotoxicity CYP3A4 substrates (astemizole, cisapride, pimozide, quinidine, terfenadine): Increased plasma levels of these , which may lead to prolonged QT interval and, rarely, torsades de pointes ergot alkaloids (ergotamine, dihydroergotamine): May increase plasma level of ergot alkaloids, leading to ergotism HIV protease inhibitors (amprenavir, nelfinavir, ritonavir, saquinavir), non-nucleoside reverse transcriptase inhibitors (delavirdine, efavirenz): Possibly inhibited metabolism of these and voriconazole methadone: Increased plasma level of methadone, possibly leading to toxicity, including QT-interval prolongation oral contraceptives: Increased plasma voriconazole level and risk of toxicity
rifabutin: Increased rifabutin plasma level; decreased voriconazole plasma level
St. John’s wort: Decreased plasma voriconazole level sulfonylureas: Possibly increased plasma level of sulfonylureas and increased risk of hypoglycemia vinca alkaloids: Possibly increased risk of neurotoxicity

Side Efect

CNS: Chills, dizziness, fever, hallucinations, headache
CV: Chest pain, hypertension, hypotension, peripheral edema, tachycardia, vasodilation
EENT: Abnormal or blurred vision, altered or enhanced visual perception, change in color perception, chromatopsia, dry mouth, eye hemorrhage, photophobia, visual disturbances
GI: Abdominal pain, diarrhea, elevated liver function test results, nausea, pancreatitis, vomiting
GU: Abnormal kidney function, acute renal failure, elevated serum creatinine level
HEME: Anemia, leukopenia, pancytopenia, thrombocytopenia
RESP: Respiratory disorders
SKIN: Cholestatic jaundice, erythema multiforme, jaundice, maculopapular rash, photosensitivity, pruritus, rash, StevensJohnson syndrome, toxic epidermal necrolysis
Other: Anaphylaxis (I.V. form), elevated alkaline phosphatase, hypokalemia, hypomagnesemia, sepsis

Cautions

Use voriconazole cautiously in patients hypersensitive to other azoles and in patients at risk for proarrhythmic events (such as those receiving cardiotoxic chemotherapy or those who have cardiomyopathy or hypokalemia) because some azoles may prolong the QT interval.

Determine if patient has any problems with galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption before starting therapy because voriconazole tablets contain lactose and shouldn’t be given to patients with these conditions.

Obtain specimens for fungal culture and other relevant laboratory studies (including histopathology), as ordered, before giving first dose. Expect to begin drug before test results are known.

Assess patient’s liver function, including bilirubin, as ordered, at the start of voriconazole therapy and periodically thereafter. Be aware that drug may be discontinued if liver abnormalities occur.

Check patient’s electrolyte levels and correct any imbalances, as ordered, before giving voriconazole because electrolyte imbalances increase the risk of adverse reactions.

For I.V. infusion, reconstitute powder with 19 ml water for injection to obtain 20 ml of concentrate containing 10 mg/ml voriconazole. To make sure exact amount of water is injected into vial, use a standard 10-ml non-automated syringe. Shake vial until all powder is dissolved. Further dilute so final concentration is no less than 0.5 mg/ml and no more than 5 mg/ml. This requires withdrawing and discarding at least an equal volume of diluent from infusion bag or bottle before instillation of concentrate.

Discard partially used vials after mixing. If infusion isn’t administered immediately, store at 2° to 8° C (37° to 46° F) for no longer than 24 hours.

Administer I.V. infusion over 1 to 2 hours at no more than 3 mg/kg/hr.

Monitor renal function, especially serum creatinine level, when giving I.V. form of voriconazole because drug may accumulate in body when creatinine clearance is less than 50 ml/min/1.73 m2, increasing the risk of

Side Efect

.
WARNING Observe patient receiving I.V. voriconazole closely for anaphylactoidtype reactions—such as flushing, fever, sweating, tachycardia, chest tightness, dyspnea, faintness, nausea, pruritus, and rash—which may occur immediately after starting infusion. Stop infusion if these reactions occur, and notify prescriber immediately.

Monitor patient closely throughout therapy for rash, which may indicate a serious cutaneous reaction, such as StevensJohnson syndrome. If rash occurs, notify prescriber, and expect that voriconazole may be discontinued.

Monitor cyclosporine, tacrolimus, and warfarin closely for elevated levels when voriconazole is given with any of these .

Monitor diabetic patients also taking sulfonylureas closely for hypoglycemia, and check blood glucose levels regularly.

Voriconazole dosage will need to be adjusted when given with phenytoin. Expect to monitor plasma phenytoin level and observe patient closely for phenytoinrelated

Side Efect

.

Assess patient’s visual function, including visual acuity, visual field, and color perception, if voriconazole therapy continues longer than 28 days.

Monitor patient closely for pancreatitis, especially if patient is a child or has risk factors for acute pancreatitis, such as recent chemotherapy or hematopoietic stem cell transplantation.

PATIENT SAFTY

Instruct patient taking oral voriconazole to take the tablets at least 1 hour before or 1 hour after a meal.

Inform female patient of possible fetal risk, and stress need to avoid pregnancy. Tell her to use effective contraception during therapy and to notify prescriber immediately if pregnancy is suspected.

Caution patient not to drive at night and to avoid hazardous activities because drug may cause visual disturbances, including blurring or photophobia.

Advise patient to avoid exposure to direct sunlight or UV light and to wear sunscreen when outdoors.

Category

Chemical class: Coumarin derivative
Therapeutic class: Anticoagulant

Pregnancy category: X

Indications

To prevent or treat pulmonary embolism; recurrent MI; thromboembolic complications from atrial fibrillation, heart valve replacement, or MI; and venous thrombosis (and its extension)
Adults.Initial: 2 to 5 mg daily for 2 to 4 days. Usual: 2 to 10 mg daily based on target PT and INR results. Maximum: Determined by target PT and INR results, as prescribed.
I.V.INJECTION
Adults.Initial: 2 to 5 mg daily infused over 1 to 2 min. Usual: 2 to 10 mg daily infused over 1 to 2 min. Maximum: Determined by target PT and INR results, as prescribed.
DOSAGE ADJUSTMENT For patients with hepatic dysfunction, dosage reduced to 0.1 mg/kg, as prescribed. For elderly patients, dosage possibly reduced based on PT and INR results.

Mechanism of Action

Interferes with the liver’s ability to synthesize vitamin K–dependent clotting factors, depleting clotting factors II (prothrombin), VII, IX, and X. This action, in turn, interferes with the clotting cascade. By depleting vitamin K–dependent clotting factors and interfering with the clotting cascade, warfarin prevents coagulation.

Incompatibilities

Don’t mix warfarin in solution with amikacin sulfate, epinephrine hydrochloride, metaraminol tartrate, oxytocin, promazine hydrochloride, tetracycline hydrochloride, or vancomycin hydrochloride.

Contraindications

Bleeding or bleeding tendencies; blood dyscrasias; cerebral or dissecting aneurysm; cerebrovascular hemorrhage; diverticulitis; eclampsia or preeclampsia; history of warfarin-induced necrosis; hypersensitivity to warfarin or its components; malignant or severe uncontrolled hypertension; malnutrition and emaciation; mental state or condition that leads to lack of patient cooperation; pericardial effusion; pericarditis; polyarthritis; pregnancy; prostatectomy; recent or planned neurosurgery, ophthalmic surgery, or spinal puncture; severe hepatic or renal disease

Interactions

acetaminophen, agrimony, aminoglycosides, amiodarone, androgens, argatroban, beta blockers, bivalirudin, capecitabine, cephalosporins, chloral hydrate, chloramphenicol, chlorpropamide, cimetidine, clofibrate, corticosteroids, cyclophosphamide, dextrothyroxine, diflunisal, disulfiram, erythromycin, ezetimibe, fluconazole, gemfibrozil, glucagon, hydantoins, ifosfamide, influenza virus vaccine, isoniazid, ketoconazole, lepirudin, loop diuretics, lovastatin, metronidazole, miconazole, mineral oil, moricizine, nalidixic acid, NSAIDs, omeprazole, penicillins, phenylbutazones, propafenone, propoxyphene, quinidine, quinine, quinolones, salicylates, streptokinase, sulfamethoxazole-trimethoprim, sulfinpyrazone, sulfonamides, tamoxifen, tetracyclines, thyroid hormones, urokinase, valdecoxib, vitamin E: Increased anticoagulant effect of warfarin, increased risk of bleeding aminoglutethimide, barbiturates, carbamazepine, cholestyramine, dicloxacillin, estrogens, ethchlorvynol, etretinate, glutethimide, griseofulvin, nafcillin, oral contraceptives, rifampin, spironolactone, sucralfate, thiazide diuretics, trazodone, vitamin C, vitamin K: Decreased anticoagulant effect of warfarin atorvastatin, pravastatin: Increased or decreased anticoagulant effect of warfarin herbal remedies (including bromelains, danshen, dong quai, garlic, ginkgo biloba, and ginseng): Increased anticoagulant effect of warfarin, increased risk of bleeding I.V. lipid emulsion, other medical products that contain soybean oil: Possibly decreased vitamin K absorption and increased anticoagulant effect of warfarin nicotine patch: Altered response to warfarin certain multivitamins, enteral feedings, vitamin K–rich : Decreased warfarin effects
alcohol use: Increased risk of hypoprothrombinemia smoking, smoking cessation: Altered response to warfarin

Side Efect

CNS: Coma, intracranial hemorrhage, loss of consciousness, syncope, weakness
CV: Angina, chest pain, hypotension
EENT: Epistaxis, intraocular hemorrhage
GI: Abdominal cramps and pain, diarrhea, hepatitis, nausea, vomiting GU:Hematuria, vaginal bleeding (abnormal)
HEME: Anemia, potentially fatal hemorrhage (from any tissue or organ)
SKIN: Alopecia, ecchymosis, jaundice, petechiae, pruritus, purple-toe syndrome, tissue necrosis
Other: Anaphylaxis

Cautions

Reconstitute parenteral warfarin just before administration with 2.7 ml sterile water for injection to yield 2 mg/ml. Then give slowly over 1 to 2 minutes through peripheral I.V.

Expect to give another parenteral anticoagulant, such as heparin or enoxaparin, with oral warfarin for at least 3 days, or until desired response occurs, before giving warfarin only.

Avoid I.M. injections during warfarin therapy, if possible, because they can result in bleeding, bruising, and hematoma.

Monitor INR (daily in acute care setting) and assess for therapeutic effects, as prescribed. Therapeutic INR levels are 2.0 to 3.0 for bioprosthetic heart valve, nonvalvular atrial fibrillation, and venous thromboembolism, and 2.5 to 3.5 after MI and for mechanical heart valve.

Expect treatment to last up to 12 weeks for bioprosthetic heart valve, 1 to 3 months for nonvalvular atrial fibrillation or venous thromboembolism, and for rest of life after MI and for mechanical heart valve replacement.
WARNING Be aware of the increased risk for intracranial hemorrhage if patient has cerebral ischemia (such as recent transient ischemic attack or minor ischemic stroke) and INR of 3 to 4.5. As prescribed, withhold next warfarin dose and give vitamin K if INR exceeds 4 because of the risk of bleeding.

Assess for occult bleeding if patient receives I.V. lipid emulsion or other medical product that contains soybean oil. Such products can decrease vitamin K absorption and increase warfarin’s anticoagulant effect.

PATIENT SAFTY

Explain that warfarin therapy aims to prevent thrombosis by decreasing clotting ability while avoiding the risk of spontaneous bleeding.

Instruct patient to take drug exactly as prescribed at the same time each evening.

Urge patient to keep weekly follow-up appointments for blood tests after discharge until PT and INR levels are stabilized.

Advise patient to avoid alcohol during warfarin therapy.

Urge patient to take precautions against bleeding, such as using an electric shaver and a soft-bristled toothbrush.Advise him to continue these precautions for 2 to 5 days after therapy stops, as directed, because anticoagulant effect may persist during this time.

Caution patient to avoid activities that could cause traumatic injury and bleeding.

Advise patient to eat consistent amounts of vitamin K–rich , such as dark green, leafy vegetables.

Urge patient to notify prescriber immediately about unusual bleeding and any unexplained symptoms, such as abnormal vaginal bleeding; dizziness; easy bruising; gum bleeding; headache; nosebleeds; prolonged bleeding from cuts; red, black, or tarry stool; red or dark brown urine; swelling; and weakness.

Advise patient to consult prescriber before taking other —including OTC and herbal remedies—during therapy.

Instruct female patient of childbearing age to stop taking warfarin and notify prescriber immediately if she is or could be pregnant.

Explain that drug may cause reversible purple-toe syndrome and that this syndrome isn’t harmful.

Urge patient to carry medical identification that reveals he’s taking warfarin.

Category

Chemical class: Peptide leukotriene receptor antagonist
Therapeutic class: Antiasthmatic

Pregnancy category: B

Indications

To treat chronic asthma

Mechanism of Action

Inhibits the selective binding of cysteinyl leukotrienes (arachidonic acid derivatives that usually mediate inflammation in asthma and other inflammatory disorders) by competitively blocking receptor sites. This action causes bronchial relaxation and decreases vascular leakage and edema, mucus secretion, eosinophil movement, and bronchial hyperresponsiveness.

Contraindications

Hypersensitivity to zafirlukast or its components

Interactions

alprazolam, amitriptyline, calcium channel blockers, carbamazepine, citalopram, corticosteroids, cyclosporine, diazepam, diclofenac, ibuprofen, imipramine, irbesartan, lidocaine, lovastatin, midazolam, phenytoin, quinidine, simvastatin, tolbutamide, tolterodine, triazolam: Inhibited metabolism and, possibly, additive adverse effects of these aspirin: Increased blood zafirlukast level erythromycin, terfenadine: Decreased response to zafirlukast
sildenafil: Increased adverse sildenafil effects
theophylline: Decreased zafirlukast level
warfarin: Prolonged PT any food: Possibly decreased bioavailability of zafirlukast

Side Efect

CNS: Asthenia, dizziness, fever, headache, insomnia, malaise
GI: Abdominal pain, diarrhea, elevated liver function test results, hepatic failure, indigestion, nausea, vomiting
MS: Back pain, myalgia
SKIN: Pruritus
Other: Generalized pain

Cautions

Zafirlukast shouldn’t be used to treat bronchospasm during an acute asthma attack or status asthmaticus; it can’t relieve symptoms quickly enough.

Assess respiratory rate, depth, and quality as well as breath sounds before and during treatment to evaluate response to therapy.

If patient is being weaned from corticosteroids while taking zafirlukast, monitor her for Churg-Strauss syndrome, a rare allergic reaction characterized by eosinophilia, fever, myalgia, weight loss, as cardiac complications, neuropathy, and worsening pulmonary symptoms.

PATIENT SAFTY

Instruct patient to take drug exactly as prescribed, in evenly spaced doses, every day, even during symptom-free periods and acute exacerbations.

Instruct patient to take drug on an empty stomach at least 1 hour before or 2 hours after meals.

Urge patient to continue using prescribed rescue inhalants for acute asthma attacks.

Teach patient how to use peak-flow meter to monitor pulmonary function.

Tell patient to immediately report evidence of liver dysfunction, such as right upper-quadrant abdominal pain, nausea, fatigue, lethargy, pruritus, jaundice, flulike symptoms, and anorexia.

Category

Chemical class: Imidazopyridine derivative
Therapeutic class: Sedative-hypnotic

Pregnancy category: C

Controlled substance schedule: IV

Indications

Short-term treatment of insomnia Adults up to age 65. 10 mg daily at bedtime, as prescribed, for up to 35 days. Usual: 10 mg daily at bedtime for 7 to 10 days. Maximum: 20 mg daily.
DOSAGE ADJUSTMENT For patients who are elderly, have hepatic impairment, or take cimetidine, dosage possibly reduced to 5 mg daily.

Mechanism of Action

Selectively binds with type 1 benzodiazepine (BZ1 or omega1) receptors on the gamma-aminobutyric acid-A receptor complex. This binding produces muscle relaxation and sedation as well as antianxiety and anticonvulsant effects.

Contraindications

Hypersensitivity to zaleplon or its components

Interactions

amitriptyline; amoxapine; azatadine; benzodiazepines; brompheniramine; chlorpheniramine; clemastine; clomipramine; clozapine; cyproheptadine; dexchlorpheniramine; diphenhydramine; doxepin; entacapone; haloperidol; hydroxyzine; imipramine; maprotiline; mirtazapine; molindone; nefazodone; nortriptyline; olanzapine; opioid analgesics; other anxiolytics, sedatives, and hypnotics; phenindamine; phenothiazines; pimozide; pramipexole; promethazine; quetiapine; risperidone; ropinirole; thioridazine; trazodone; trimipramine; tripelennamine: Possibly additive CNS depression carbamazepine, phenobarbital, phenytoin,
rifampin: Reduced zaleplon effects
cimetidine: Increased blood zaleplon level
flumazenil: Reversal of zaleplon’s sedation high-fat : Prolonged absorption time and reduced effectiveness of zaleplon
alcohol use: Increased CNS depression

Side Efect

CNS: Amnesia, anxiety, complex behaviors (such as sleep driving), depression, dizziness, drowsiness, fever, hallucinations, hypertonia, insomnia, paresthesia, seizures, suicidal ideation, tremor, vertigo
EENT: Dry mouth, gingivitis, glossitis, mouth ulcers, stomatitis, throat tightness
GI: Anorexia, colitis, constipation, eructation, esophagitis, flatulence, gastritis, gastroenteritis, increased appetite, indigestion, melena, nausea, rectal bleeding, vomiting
MS: Back pain
RESP: Dyspnea
SKIN: Photosensitivity, pruritus, rash
Other: Anaphylaxis, angioedema, physical and psychological dependence

Cautions

Give zaleplon just before bedtime because its onset of action is rapid.

Avoid giving drug with or after a heavy, high-fat meal because decreased absorption may reduce drug’s effects.

Watch patient closely for suicidal tendencies, particularly when therapy starts and dosage changes, because depression may worsen temporarily during these times, possibly leading to suicidal ideation.

Monitor patient for signs of drug abuse because zaleplon has an abuse potential similar to that of benzodiazepines and benzodiazepine-like hypnotics.
WARNING Monitor patient closely for hypersensitivity reactions, such as dyspnea, throat tightness, nausea, vomiting, and swelling. If present, discontinue zaleplon immediately, notify prescriber, and provide supportive care.

PATIENT SAFTY

Explain that zaleplon is intended for short-term use. Advise against using it for any condition other than insomnia.

Caution patient against exceeding prescribed dosage.

Instruct patient to take zaleplon immediately before bedtime or right after having trouble falling asleep because of drug’s rapid onset of action.

Teach patient alternative measures for relaxation and sleep induction.

Advise patient to consult prescriber before taking other CNS depressants.

Urge patient to avoid alcohol during zaleplon therapy because it increases risk of abnormal behaviors, such as sleep driving.

Warn patient that zaleplon contains FD & C Yellow No. 5 (tartrazine), which can cause an allergic reaction, especially in those with an aspirin sensitivity. Instruct patient to report allergic reactions, such as rash or difficulty breathing, to prescriber.

Instruct patient to notify prescriber if inability to sleep continues. Dosage may need to be adjusted.

Instruct patient to stop taking zaleplon and seek emergency care if she has trouble breathing, throat tightness, nausea, vomiting, or abnormal swelling.

Explain that drug may cause abnormal behaviors during sleep, such as driving a car, eating, talking on the phone, or having sex without any recall of the event. If family notices any such behavior or patient sees evidence of such behavior upon awakening, prescriber should be notified.

Urge family or caregiver to watch patient closely for suicidal tendencies, especially when therapy starts or dosage changes.

Category

Chemical class: 25 amino acid polybasic peptide
Therapeutic class: Analgesic

Pregnancy category: C

Indications

To manage severe chronic pain in patients intolerant of or refractory to other pain management measures

INTRATHECAL

Adults.Initial: 2.4 mcg daily (0.1 mcg/hr), increased as needed by 2.4 mcg daily but no more than 3 times/wk. Maximum: 19.2 mcg/ day (0.8 mcg/hr) by day 21.

Contraindications

History of psychosis; hypersensitivity to ziconotide or its components; conditions or treatment that make intrathecal use hazardous (infection at microinfusion site, uncontrolled bleeding diathesis, spinal canal obstruction that impairs CSF circulation).

Interactions

CNS depressants: Increased risk of adverse CNS reactions

Side Efect

CNS: Abnormal gait, agitation, anxiety, aphasia, asthenia, ataxia, chills, confusion, CSF abnormality, decreased reflexes, depression, difficulty concentrating, dizziness, dysesthesia, emotional lability, fever, hallucinations, headache, hostility, hyperesthesia, hypertonia, incoordination, insomnia, malaise, memory loss, meningitis, nervousness, neuralgia, paranoia, paresthesia, psychosis, seizures, somnolence, speech disorder, stroke, stupor, suicidal ideation, syncope, tremor, twitching, unusual dreams, vertigo
CV: Atrial fibrillation, bradycardia, chest pain, edema, hypertension, hypotension, orthostatic hypotension, peripheral edema, tachycardia, T-wave changes on ECG, vasodilation
EENT: Abnormal vision, diplopia, dry mouth, nystagmus, pharyngitis, photophobia, rhinitis, sinusitis, taste perversion, tinnitus
GI: Abdominal pain, anorexia, constipation, diarrhea, indigestion, nausea, vomiting
GU: Acute renal failure, dysuria, urinary hesitancy or incontinence, urine retention, UTI
HEME: Anemia
MS: Arthralgia, arthritis, back pain, leg cramps, muscle spasms or weakness, myalgia, myasthenia, neck pain or rigidity, rhabdomyolysis
RESP: Aspiration pneumonia, bronchitis, cough, dyspnea, lung disorder, pneumonia, respiratory distress
SKIN: Cellulitis, diaphoresis, dry skin, ecchymosis, pruritus, rash
Other: Catheter site infection or pain, dehydration, elevated CK level, flulike symptoms, generalized pain, hypokalemia, sepsis, viral infection, weight loss

Cautions

Determine if patient will receive ziconotide therapy by implanted variable-rate microinfusion device or by external microinfusion device and catheter. Then, follow manufacturer guidelines for programming the microinfusion devise and doing an initial pump fill, including priming using only undiluted 25-mcg/ml solution and rinsing the internal pump surfaces with 2 ml of drug three times.

Use strict aseptic technique when preparing ziconotide solution and filling, refilling, or handling the microinfusion device.

Be aware that initial ziconotide dosage shouldn’t exceed 2.4 mcg daily.

Know that refills can use diluted or undiluted ziconotide solutions. If diluting ziconotide, use only normal saline solution without preservatives, following manufacturer guidelines. Refrigerate solution up to 24 hours if it isn’t used immediately. Expect device to need refilling about every 40 days if ziconotide is given diluted or about 60 days if given undiluted.

Assess patient’s response to ziconotide regularly. Notify prescriber if pain relief isn’t adequate, and expect to increase dosage.

Check infusion site regularly, and be aware that meningitis can occur within 24 hours after contamination of delivery system; a disconnected catheter is the most common problem with external devices.

Monitor patient closely for evidence of meningitis, such as headache, stiff neck,

Mechanism of Action

Pain sensations are transmitted by sensory neurons that travel through N-type calcium channels in the dorsal horn of the spinal cord and ascend to the brain, as shown below. Ziconotide binds to N-type calcium channels on primary nociceptive afferent nerves in superficial layers of the dorsal horn, as shown below. By blocking these channels the drug prevents excitatory neurotransmitter release in primary afferent nerve terminals and relieves pain. altered mental status, nausea, vomiting, and occasionally seizures caused by inadvertent contamination of microinfusion device or catheter tract used to deliver ziconotide. Notify prescriber immediately if you suspect meningitis.

Monitor patient closely for cognitive impairment, hallucinations, or changes in mood or consciousness because ziconotide may cause severe psychiatric symptoms and neurologic impairment. If present, notify prescriber and expect to decrease dosage or stop ziconotide. Provide supportive care, as prescribed, for adverse effects. Tell prescriber again if adverse effects are still present after 2 weeks.

Expect to stop ziconotide temporarily if patient becomes unresponsive or stuporous during therapy; drug may be continued when patient reverts to previous mental status.

Ziconotide can be stopped abruptly without causing withdrawal symptoms.

Monitor patient’s serum CK level every other week for first month of therapy and monthly thereafter, as ordered. If levels become elevated, notify prescriber and expect to decrease ziconotide dosage or stop drug until levels return to normal.

PATIENT SAFTY

Teach caregiver how to care for external device, if present. Stress the need for strict aseptic technique with the microinfusion device and connections and the need to check the site often for problems, such as a disconnected catheter, which increase the risk of meningitis.

Review evidence of meningitis with caregiver, and tell her to contact prescriber immediately if she suspects meningitis.

Advise patient to notify prescriber if pain relief isn’t adequate.

Tell patient and caregiver to notify prescriber immediately about muscle pain, soreness, and weakness with or without dark urine or a change in mental status or mood, including depression or suicidal ideation.

Advise patient to avoid hazardous activities that require mental alertness or motor coordination while receiving ziconotide.

Caution patient to avoid taking OTC preparations that contain CNS depressants because of the risk of adverse CNS effects.

Category

Chemical class: Leukotriene inhibitor
Therapeutic class: Antiasthmatic

Pregnancy category: C

Indications

To prevent or treat chronic asthma

Mechanism of Action

Inhibits formation of leukotrienes found mainly in neutrophils, eosinophils, monocytes, macrophages, and mast cells. Normally, leukotrienes augment neutrophil and eosinophil migration, neutrophil and monocyte aggregation, leukocyte adhesion, capillary permeability, and smooth-muscle contraction. By inhibiting leukotriene formation, zileuton causes bronchial relaxation and decreases vascular leakage and edema, mucus secretion, eosinophil movement, and bronchial hyperresponsiveness.

Contraindications

Hepatic impairment, hypersensitivity to zileuton or its components

Interactions

propranolol, terfenadine: Increased effects of these
theophylline: Doubled theophylline level
warfarin: Prolonged PT and INR

Side Efect

CNS: Asthenia, dizziness, fever, headache, hypertonia, insomnia, malaise, nervousness, neuropsychiatric events, sleep disorders, somnolence
CV: Chest pain
EENT: Conjunctivitis
GI: Abdominal pain, constipation, flatulence, indigestion, nausea, vomiting
GU: UTI, vaginitis
MS: Arthralgia,myalgia,neck pain or rigidity
SKIN: Pruritus, rash, urticaria
Other: Lymphadenopathy

Cautions

Zileuton shouldn’t be used to treat bronchospasm during an acute asthma attack or status asthmaticus; it can’t relieve symptoms quickly enough.

Monitor serum ALT level, as ordered, usually before treatment starts, once a month for 3 months, every 2 to 3 months for remainder of first year, and periodically thereafter during therapy.

Monitor results of liver and pulmonary function tests and CBC during therapy.

Monitor patient taking zileuton for neurospychiatric symptoms including worsening of pre-existing psychiatric illness. If present, notify prescriber immediately, institute safety measures and expect drug to be discontinued.

PATIENT SAFTY

Advise patient to take drug exactly as prescribed, in evenly spaced doses, every day. Stress need to take drug even during symptom-free periods and acute exacerbations.

Urge patient not to chew, cut, or crush capsule but to swallow it whole.

Instruct patient to continue using rescue inhalants, as prescribed, for acute attacks.

Teach patient how to use peak-flow meter to assess and monitor pulmonary function.

Instruct patient to report any abnormal thoughts or behavior.

Category

Chemical class: Trace element, mineral
Therapeutic class: Copper absorption inhibitor, nutritional supplement Pregnancy category: A (oral), C (I.V.)

Indications

To prevent zinc deficiency based on U.S. and Canadian recommended daily allowances , , LOZENGES, Men and boys age 11 and over.15 mg (9 to 12 mg Canadian) elemental zinc daily. Women and girls age 11 and over. 12 mg (9 mg Canadian) elemental zinc daily. Pregnant women. 15 mg (15 mg Canadian) elemental zinc daily. Breast-feeding women.16 to 19 mg (15 mg Canadian) elemental zinc daily. Children ages 7 to 10. 10 mg (7 to 9 mg Canadian) elemental zinc daily. Children ages 4 to 6. 10 mg (5 mg Canadian) elemental zinc daily. Children from birth to age 3. 5 to 10 mg (2 to 4 mg Canadian) elemental zinc daily.

IV

Adults and children. 2.5 to 4 mg daily added to total parenteral nutrition (TPN) solution. Maximum: 12 mg daily. Children from birth to age 5. 100 mcg/kg daily added to TPN solution. Premature infants weighing up to 3 kg. 300 mcg/kg daily added to TPN solution. To treat zinc deficiency , , LOZENGES, Adults and children. Dosage individualized based on severity of deficiency.

IV

Adults and adolescents. 2.5 to 4 mg daily added to TPN solution. Maximum: 12 mg daily. Children from birth to age 5. 100 mcg/kg daily added to TPN solution. Premature infants weighing up to 3 kg. 300 mcg/kg daily added to TPN solution. As adjunct maintenance therapy for patients previously treated for Wilson’s disease
Adults.50 mg t.i.d. Pregnant women. 25 mg t.i.d., increased to 50 mg t.i.d. if drug effectiveness decreases. Children age 10 and over. 25 mg t.i.d., increased to 50 mg t.i.d. if drug effectiveness decreases.

Mechanism of Action

Needed for proper function of more than 200 metalloenzymes (those with tightly bound zinc atoms as an integral part of their structure), including carbonic anhydrase, carboxypeptidase A, alcohol dehydrogenase, alkaline phosphatase, and RNA polymerase. Zinc also helps maintain nucleic acid, protein, and cell membrane structure and is essential for certain physiologic functions, including cell growth and division, sexual maturation and reproduction, dark adaptation and night vision, wound healing, host immunity, and taste acuity. This mineral also provides cellular antioxidant protection by scavenging free radicals. In addition, zinc acetate interferes with intestinal absorption of copper and produces a protein that binds with copper, preventing its transfer to blood. Bound copper is then excreted in stools, thus decreasing copper toxicity in Wilson’s disease.

Contraindications

Hypersensitivity to zinc or its components

Interactions

copper supplements: Impaired copper absorption (with large doses of zinc) oral iron supplements, oral phosphate salts, penicillamine, phosphorus-containing : Decreased zinc absorption quinolones, tetracyclines: Decreased absorption and possibly decreased effectiveness of these antibiotics thiazide diuretics: Increased urinary excretion of zinc zinc-containing preparations: Increased blood zinc level fiberor phylate-containing (such as bran, whole-grain breads, cereal), phosphorus-containing (including milk, poultry): Decreased zinc absorption

Cautions

WARNING Don’t give I.V. zinc preparations that contain benzyl alcohol to neonates or premature infants because this preservative may cause a fatal toxic syndrome characterized by metabolic acidosis and CNS, respiratory, circulatory, and renal function impairment.

Give oral zinc supplements 1 hour before or 2 to 3 hours after meals; at least 2 hours after giving oral iron supplements (to prevent decreased zinc absorption) or copper supplements (to prevent decreased copper absorption); and at least 6 hours before or 2 hours after administering quinolone or tetracycline antibiotics (to prevent decreased absorption of these ).

Monitor patient receiving long-term zinc therapy for sideroblastic anemia, which may result from zinc-induced copper deficiency and is characterized by anemia, leukopenia, neutropenia, granulocytopenia, and bone marrow problems. Be aware that these effects are reversible after zinc is discontinued.

Monitor patient with preexisting copper deficiency for exacerbation of this condition; zinc can decrease serum copper level.

Assess for signs and symptoms of zinc deficiency, such as growth retardation, hypogonadism, delayed sexual maturation, alopecia, impaired wound healing, skin lesions, immune deficiencies, behavioral disturbances, night blindness, and impaired sense of taste.

Monitor blood alkaline phosphatase (ALP) level monthly, as ordered; it may increase.

Be aware that zinc chloride contains aluminum, which may accumulate to the point of toxicity if patient’s kidney function is impaired. Assess kidney function regularly.

PATIENT SAFTY

Explain the need for a zinc supplement.

Instruct patient to take zinc on an empty stomach, at least 1 hour before or 2 hours after meals. Caution her not to take zinc within 2 hours of iron or copper supplements or phosphorus-containing .

Instruct patient to let zinc lozenge dissolve in mouth slowly and completely and not to swallow it whole or chew it. Advise her not to take zinc lozenges more often than directed.

Category

Chemical class: Benzisoxazole derivative
Therapeutic class: Antipsychotic

Pregnancy category: C

Indications

To treat schizophrenia
Adults.Initial: 20 mg b.i.d. Dosage increased as indicated every 2 or more days. Usual: 20 to 80 mg b.i.d. Maximum: 100 mg b.i.d.

IM

Adults. Initial: 10 to 20 mg. 10 mg dose may be given every 2 hr up to maximum dose; 20 mg dose may be given every 4 hr up to maximum dose. Maximum: 40 mg daily. To treat acute manic or mixed episodes of bipolar disorder
Adults. Initial: 40 mg b.i.d. with food on day 1; then increased to 60 or 80 mg on day 2 with further adjustments as needed. As adjunct to lithium or valproate for maintenance treatment of bipolar I disorder
Adults.Same dose patient was initially stabilized on that falls within 40 mg to 80 mg twice daily.

Mechanism of Action

Selectively blocks serotonin and dopamine receptors in the mesocortical tract of the CNS, thereby suppressing psychotic symptoms.

Incompatibilities

Don’t mix injection form with or solvents other than sterile water for injection.

Contraindications

Concurrent use of other that prolong QT interval, history of arrhythmia, hypersensitivity to ziprasidone or its components, history of prolonged QT interval, recent acute MI, uncompensated heart failure

Interactions

antihypertensives: Additive antihypertensive effects carbamazepine: Possibly decreased blood ziprasidone level
CNS depressants: Increased CNS depression dopamine agonists, levodopa: Decreased therapeutic effects of these that prolong QT interval (including quinidine, dofetilide, pimozide, sotalol, thioridazine, and sparfloxacin): Increased risk of prolonged QT or QTc interval, torsades de pointes, and sudden death
ketoconazole: Possibly increased blood ziprasidone level all : Increased ziprasidone absorption

Side Efect

CNS: Agitation, akathisia, amnesia, anxiety, asthenia, CVA, depression, dizziness, dystonia, extrapyramidal reactions, headache, hypertonia, hypomania, insomnia, mania, neuroleptic malignant syndrome, paresthesia, personality or speech disorder, serotonin syndrome, somnolence, syncope, suicidal ideation, tardive dyskinesia, tremor
CV: Bradycardia, chest pain, hypercholesterolemia, hypertension, orthostatic hypotension, prolonged QT or QTc interval, tachycardia, thrombophlebitis, vasodilation
EENT: Abnormal vision, dry mouth, increased salivation, rhinitis, tongue swelling
ENDO: Dysmenorrhea, hyperglycemia
GI: Abdominal pain, anorexia, constipation, diarrhea, dysphagia, indigestion, nausea, rectal bleeding, vomiting
GU: Priapism, urinary incontinence
HEME: Agranulocytosis, leukopenia, neutropenia
MS: Arthralgia, back pain, dysarthria, myalgia
RESP: Cough, pulmonary embolism, upper respiratory tract infection
SKIN: Allergic dermatitis, diaphoresis, furunculosis, rash, urticaria
Other: Accidental injury, angioedema, flulike symptoms, injection site pain, weight gain

Cautions

WARNING Ziprasidone shouldn’t be used to treat elderly patients with dementia-related psychosis because drug increases the risk of death in these patients.

Protect ziprasidone vials from light. Reconstitute by adding 1.2 ml sterile water for injection to vial and shaking vigorously until drug is dissolved. Each ml of reconstituted solution contains 20 mg ziprasidone. Discard any unused portion.

Give only by I.M. route.

Reconstituted drug may be stored 24 hours protected from light or up to 7 days if refrigerated and protected from light.

Administer I.M. form cautiously to patients with impaired renal function.
WARNING Assess cardiac rhythm in patients with hypokalemia or hypomagnesemia. Dizziness, palpitations, and syncope may indicate life-threatening torsades de pointes. Be prepared to stop ziprasidone if QTc interval is greater than 500 msec.

Monitor patient, especially elderly woman, for involuntary movements, which may become irreversible tardive dyskinesia. If symptoms develop, notify prescriber immediately and be prepared to stop drug.

Immediately report evidence of neuroleptic malignant syndrome, a rare but potentially fatal adverse reaction including hyperpyrexia, muscle rigidity, altered mental status, irregular pulse, blood pressure changes, tachycardia, diaphoresis, arrhythmia, myoglobinuria (rhabdomyolysis), and acute renal failure.

Monitor patient’s blood glucose and lipid levels routinely, as ordered, because drug increases risk of hyperglycemia and hypercholesterolemia.

Monitor patient’s CBC, as ordered, because serious adverse hematologic reactions may occur, such as agranulocytosis, leukopenia, and neutropenia. Monitor more frequently during first few months of therapy if patient has a history of druginduced leukopenia, neutropenia, or significantly low WBC count. If abnormalities occur during ziprasidone therapy, watch for fever and other evidence of infection, notify prescriber, and expect to discontinue drug if severe.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

PATIENT SAFTY

Instruct patient to take ziprasidone with food to increase absorption.

Advise patient to avoid hazardous activities until CNS effects are known.

Tell family to monitor patient closely for suicidal tendencies; patients with psychotic illness or bipolar disorder are at greater risk.

Urge patient to rise slowly from seated or lying position to minimize orthostatic hypotension.

Urge patient to notify prescriber immediately if he develops any sudden onset, unusual, persistent, or servere adverse reactions.

Category

Chemical class: Bisphosphonate
Therapeutic class: Antihypercalcemic, bone resorption inhibitor

Pregnancy category: D

Indications

To treat hypercalcemia caused by cancer
IV:(ZOMETA)
Adults. 4 mg infused over at least 15 min. After 7 days, retreatment with 4 mg if serum calcium level doesn't remain at or return to normal. Maximum: 4 mg/dose. As adjunct treatment for patients with multiple myeloma or bony metastasis who are receiving standard antineoplastic therapy and have a creatinine clearance above 60 ml/min/1.73 m2
IV:(ZOMETA)
Adults. 4 mg infused over at least 15 min every 3 to 4 wk.
DOSAGE ADJUSTMENT If patient’s creatinine clearance is 50 to 60 ml/min/1.73 m2, dosage decreased to 3.5 mg; if it’s 40 to 49 ml/min/1.73 m2, dosage decreased to 3.3 mg; and if it’s 30 to 39 ml/min/1.73 m2, dosage decreased to 3 mg. To treat postmenopausal osteoporosis in women; to treat osteoporosis in men; to treat and prevent glucocorticoid-induced osteoporosis in patients receiving daily prednisone doses of 7.5 mg or greater for at least 12 months

IV

Adults.5 mg infused over at least 15 min once yearly. To treat Paget’s disease of the bone

IV

Adults. 5 mg infused over at least 15 min after 2 wk of receiving 1,500 mg elemental calcium daily in divided doses and 800 international units vitamin D daily. To prevent osteoporosis in postmenopausal women

IV

Adults.5 mg infused over at least 15 min every 2 years.

Mechanism of Action

Inhibits resorption of mineralized bone and cartilage by osteoclasts and induces osteoclast breakdown. In cancer-related hypercalcemia, hyperactive osteoclasts cause bone resorption and release of calcium into blood, which causes polyuria, GI disruption, progressive dehydration, and decreasing GFR. This, in turn, increases renal calcium resorption and worsens hypercalcemia. Zoledronic acid interrupts this process.

Incompatibilities

Don’t mix zoledronic acid with calciumcontaining I.V. solutions, such as lactated Ringer’s solution.

Contraindications

Hypersensitivity to zoledronic acid, other bisphosphonates, or their components

Interactions

aminoglycosides: Possibly additive serum calcium–lowering effect loop diuretics, such as furosemide: Possibly increased risk of hypocalcemia
NSAIDs: Increased risk of nephrotoxicity

Side Efect

CNS: Anxiety, asthenia, chills, confusion, depression, dizziness, fatigue, fever, headache, hyperesthesia, hypoesthesia, insomnia, malaise, paresthesia, tremor, vertigo, weakness
CV: Atrial fibrillation, bradycardia, chest pain, hypertension, hypotension, peripheral edema
EENT: Blurred vision, conjunctivitis, episcleritis, iritis, orbital edema or inflammation, scleritis, sore throat, stomatitis, taste disturbance, uveitis
GI: Abdominal pain, anorexia, constipation, diarrhea, dyspepsia, nausea, vomiting
GU: Elevated serum creatinine level, hematuria, proteinuria, renal insufficiency or failure, UTI
HEME: Anemia, neutropenia, thrombocytopenia
MS: Arthralgia; incapacitating bone, joint, or muscle pain; muscle spasms; myalgia; osteo-necrosis of the jaw
RESP: Bronchospasm, cough, dyspnea, upper respiratory tract infection
SKIN: Alopecia, dermatitis, flushing, urticaria
Other: Aggravated malignant neoplasm, anaphylaxis, angioedema, flulike illness, hypersensitivity reaction, hyperkalemia, hypernatremia, hypocalcemia, hypomagnesemia, hypophosphatemia, infusion site redness and swelling, weight gain

Cautions

Be aware that zoledronic acid isn’t indicated for hypercalcemia from hyperparathyroidism or other non-tumor conditions.

Use cautiously in patients with aspirin sensitivity because biphosphonates such as zoledronic acid have caused bronchoconstriction in these patients.

Make sure patient has had a dental checkup before zoledronic acid starts, especially if patient has cancer; is receiving chemotherapy, head or neck radiation, or a corticosteroid; or has poor oral hygiene because risk of osteonecrosis is increased in these patients, and invasive dental procedures during zoledronic acid therapy may worsen osteonecrosis.

Expect to aggressively hydrate hypercalcemic patient with I.V. normal saline solution before and during zoledronic acid therapy, as prescribed, to achieve and maintain urine output of about 2 L daily.
WARNING During hydration, monitor fluid intake and output often and assess patient, especially one with heart failure, for evidence of life-threatening overhydration.

Hypocalcemia and mineral metabolism disorders must be treated before zoledronic acid therapy begins.

Be aware that Reclast doesn’t need reconstitution.

Reconstitute Zometa by adding 5 ml of sterile water for injection to drug vial to yield solution that contains 4 mg of zoledronic acid. Make sure drug is completely dissolved before withdrawing prescribed dose. Further dilute in 100 ml normal saline solution or 5% dextrose injection, and infuse over no less than 15 minutes.

Before giving zoledronic acid, inspect reconstituted and diluted solution and discard it if particles or discoloration are present.

Expect to give acetaminophen, if not contraindicated, before zoledronic acid to reduce

Side Efect

, such as fever, headache, myalgia, and flulike symptoms. These reactions usually occur within first 3 days after zoledronic acid administration and resolve within 3 days (although resolution may take up to 14 days for some patients).

Refrigerate reconstituted drug at 2° to 8° C (36° to 46° F) and discard after 24 hours.

Give drug as a single I.V. solution in a separate I.V. line.
WARNING Be aware that a single dose of Zometa shouldn’t exceed 4 mg and that neither Zometa nor Reclast should be infused over less than 15 minutes because exceeding these limits may lead to significant renal function deterioration, which may progress to renal failure.
WARNING Assess patient’s renal function, as ordered, before and during zoledronic acid therapy to detect renal deterioration. For patient with a normal serum creatinine level who develops an increase of 0.5 mg/ dl within 2 weeks of receiving zoledronic acid, expect to withhold next dose until serum creatinine level is within 10% of patient’s baseline value. For patient with an abnormal serum creatinine level who develops an increase of 1.0 mg/dl within 2 weeks of receiving drug, expect to withhold next dose until serum creatinine level is within 10% of baseline value.

Monitor patient’s serum calcium, magnesium, and phosphate levels, as ordered, during zoledronic acid therapy. If hypocalcemia, hypomagnesemia, or hypophosphatemia occurs, expect to give short-term supplemental therapy.

Assess aspirin-sensitive asthma patients for worsening of respiratory symptoms during zoledronic acid therapy because other bisphosphonates have caused bronchoconstriction in these patients.

Store drug at 25° C (77° F).

PATIENT SAFTY

Teach patient the importance of consuming a nutritious diet, including adequate amounts of calcium and vitamin D.

Advise patient to alert prescriber about muscle or bone pain.

Instruct patient on proper oral hygiene and on need to notify prescriber before undergoing invasive dental procedures.

Advise women of childbearing age to notify prescriber immediately if they are or could be pregnant because drug will need to be stopped.

Category

Chemical class: Selective 5-hydroxytryptamine agonist
Therapeutic class: Antimigraine

Pregnancy category: C

Indications

To treat acute migraine headache with or without aura

Adults. 2.5 mg, repeated every 2 hr p.r.n. Maximum: 10 mg in 24 hr or three headaches/mo.
Adults. 2.5 mg or less, repeated every 2 hr p.r.n. Maximum: 10 mg in 24 hr or three headaches/mo.
NASAL SPRAY
Adults. 5 mg, repeated in 2 hr if needed. Maximum: 10 mg/24 hr.
DOSAGE ADJUSTMENT Dosage reduced to less than 2.5 mg for patients with hepatic impairment.

Mechanism of Action

Constricts inflamed and dilated cranial blood vessels in the carotid circulation and inhibits production of proinflammatory neuropeptides by binding to receptors on intracranial blood vessels and sensory nerves in the trigeminal-vascular system to stimulate negative feedback, which halts the release of serotonin.

Contraindications

Basilar or hemiplegic migraine, cardiovascular disease, concurrent use of ergotamine-containing , hypersensitivity to zolmitriptan or its components, ischemic heart disease, peripheral vascular disease, Prinzmetal’s angina, symptomatic WolffParkinson-White syndrome or other accessory pathway conduction disorder, use of another 5-hydroxytryptamine agonist within past 24 hours, use of an MAO inhibitor within 14 days

Interactions

acetaminophen: Delayed peak effect of acetaminophen (by 1 hour)
cimetidine: Prolonged zolmitriptan half-life ergot alkaloids: Prolonged vasoconstriction effects fluoxetine, fluvoxamine, paroxetine, sertraline: Hyperreflexia, lack of coordination, and weakness
MAO inhibitors: Increased zolmitriptan effects naratriptan, rizatriptan, sumatriptan: Prolonged zolmitriptan effects oral contraceptives, propranolol: Increased blood zolmitriptan level serotonin and norepinephrine reuptake inhibitors: Increased risk of developing serotonin syndrome

Side Efect

CNS: Asthenia, dizziness, hyperesthesia, paresthesia, somnolence, vertigo
CV: Angina, coronary artery vasospasm, hypertension, MI, palpitations, transient myocardial ischemia, ventricular fibrillation or tachycardia
EENT: Dry mouth, vision disturbance
GI: Abdominal pain, bloody diarrhea, dysphagia, GI or splenic infarction, indigestion, ischemic colitis, nausea, vomiting
MS: Myalgia; myasthenia; pain, pressure, or tightness in jaw, neck, or throat
SKIN: Diaphoresis, flushing
Other: Anaphylaxis, anaphylactoid reaction, angioedema

Cautions

WARNING Monitor patient for signs and symptoms of vasoconstriction, which may lead to vascular and colonic ischemia with abdominal pain and bloody diarrhea, especially if patient has peripheral vascular disease (including Raynaud’s phenomenon) or ischemic bowel disease.

Monitor elderly patients and those with hepatic impairment for increased blood pressure, and notify prescriber immediately if it occurs.

Monitor patient closely for signs and symptoms of angina. If patient develops chest pain, notify prescriber.
WARNING Monitor patient closely for signs and symptoms of serotonin syndrome, which may include agitation, hallucinations, coma, tachycardia, labile blood pressure, hyperthermia, hyperreflexia, incoordination, nausea, vomiting, and diarrhea. Notify prescriber immediately because serotonin syndrome may be life-threatening. Be prepared to provide supportive care and discontinue zolmitriptan.

PATIENT SAFTY

Urge patient to consult prescriber before treating more than three headaches in 30 days.

Advise patient not to remove disintegrating tablet from blister pack until just before taking the tablet. Instruct her to peel open pack, let tablet dissolve on her tongue, and then swallow.

Urge patient to notify prescriber about unusual or severe

Side Efect

.

Caution patient using
NASAL SPRAY to avoid spraying drug into her eyes.

Instruct patient not to take zolmitriptan within 24 hours of other in the same class.

Category

Chemical class: Imidazopyridine derivative
Therapeutic class: Antianxiety, sedativehypnotic

Pregnancy category: B

Controlled substance schedule: IV zolpidem tartrate 1104

Indications

To provide short-term treatment of insomnia


Adults. 10 mg at bedtime for 7 to 10 days. Maximum: 10 mg daily.
DOSAGE ADJUSTMENT For elderly or debilitated patients and those with hepatic impairment, dosage possibly reduced to 5 mg at bedtime, with a maximum of 5 mg daily for nursing facility residents
Adults. 12.5 mg immediately before at bedtime.
DOSAGE ADJUSTMENT For elderly or debilitated patients and those with hepatic impairment, dosage reduced to 6.25 mg immediately before at bedtime.

Mechanism of Action

May potentiate the effects of gammaaminobutyric acid (GABA) and other inhibitory neurotransmitters. By binding to specific benzodiazepine receptors in the limbic and cortical areas of the CNS, zolpidem increases GABA’s inhibitory effects, blocks cortical and limbic arousal, and preserves deep sleep (stages 3 and 4).

Contraindications

Hypersensitivity to zolpidem or its components, ritonavir therapy

Interactions

azole antifungals: Increased CNS activity and additive adverse effects of zolpidem barbiturates, chlorpromazine, general anesthetics, opioid agonists, other CNS depressants, phenothiazines, tramadol, tricyclic antidepressants: Possibly increased CNS depression and reduced psychomotor function
bupropion: Increased blood zolpidem level, possibly visual hallucinations, loss of alertness desipramine, imipramine: Increased risk of visual hallucinations and reduced alertness
flumazenil: Antagonized sedative effect
haloperidol: Increased CNS depression
nevirapine: Decreased blood zolpidem level rifabutin,
rifampin: Increased zolpidem clearance selective serotonin-reuptake inhibitors: Increased risk of delusions, disorientation, and hallucinations all : Increased time to peak blood zolpidem level, decreased effects of zolpidem
alcohol use: Increased CNS depression

Side Efect

CNS: Amnesia, asthenia, ataxia, complex behaviors (such as sleep driving), confusion, dizziness, drowsiness, euphoria, hallucinations, headache, insomnia, lethargy, paradoxical CNS stimulation (including agitation, euphoria, hallucinations, hyperactivity, and nightmares), vertigo
EENT: Diplopia, throat tightness, visual abnormality
GI: Constipation, diarrhea, hiccups, indigestion, nausea, vomiting
GU: UTI
MS: Arthralgia, myalgia
RESP: Dyspnea, upper respiratory infection
Other: Anaphylaxis, angioedema, withdrawal symptoms

Cautions

Use zolpidem cautiously in patients with additional disorders because it isn’t known if zolpidem therapy might aggravate these conditions.

Administer zolpidem just before patient’s bedtime because drug has a rapid onset of action.

Expect patient to receive no more than a 1-month supply of zolpidem for outpatient therapy.
WARNING If zolpidem is withdrawn abruptly (especially after prolonged therapy), monitor patient for withdrawal symptoms, such as abdominal cramps or discomfort, fatigue, flushing, inconsolable crying, light-headedness, nausea, nervousness, panic attack, rebound insomnia, and vomiting.

Expect that zolpidem will produce anticonvulsant and muscle relaxant effects at high doses.

If patient takes other CNS depressants, expect to reduce zolpidem dosage, as prescribed.
WARNING Monitor patient closely for hypersensitivity reactions such as dyspnea, throat tightness, nausea, vomiting, and swelling. If present, discontinue zolpidem immediately, notify prescriber, and provide supportive care.

PATIENT SAFTY

Caution patient to take drug exactly as prescribed and not to increase dosage unless directed by prescriber.

Advise patient taking extended-release form to swallow tablet whole and not to break, crush, or chew it.

Advise patient taking orally disintegrating form to place tablet on tongue, let it dissolve, and then swallow with saliva or, if patient prefers, with water.

Instruct patient to take zolpidem immediately before going to bed, on an empty stomach.

Advise patient to notify prescriber immediately about abdominal cramps or discomfort, fatigue, flushing, inconsolable crying, light-headedness, nausea, nervousness, panic attack, and vomiting.

Instruct patient to stop taking zolpidem and seek emergency care if she has trouble breathing, throat tightness, nausea, vomiting, or abnormally swelling.

Advise patient that zolpidem may produce abnormal behaviors during sleep, such as driving a car, eating, talking on the phone, or having sex without any recall of the event. If patient’s family notices any such behavior or if patient sees evidence of such behavior upon awakening, prescriber should be notified.

Category

Chemical class: Benzisoxazole derivative, sulfonamide
Therapeutic class: Anticonvulsant

Pregnancy category: C

Indications

As adjunct to treat partial seizures
Adults.Initial: 100 mg daily. Dosage increased by 100 mg daily every 2 wk, as needed. Usual: 200 to 400 mg daily. Maximum: 600 mg daily.

Mechanism of Action

May stop seizures and suppress their foci by blocking sodium channels and reducing voltage-dependent, inward currents from calcium channels. This action stabilizes neuronal membranes and suppresses synchronized neuronal hyperactivity.

Contraindications

Hypersensitivity to sulfonamides, zonisamide, or their components

Interactions

carbamazepine, phenobarbital, phenytoin, valproate: Possibly decreased blood zonisamide level
CNS depressants: Additive CNS depressant effects grapefruit juice: Possibly decreased metabolism of zonisamide

Side Efect

CNS: Agitation, ataxia, dizziness, irritability, somnolence, suicidal ideation
GI: Anorexia
Other: Metabolic acidosis

Cautions

Obtain a serum bicarbonate level before startsing zonisamide and then periodically during therapy, as prescribed because drug may cause metabolic acidosis, especially in patients with predisposing conditions or therapies or who are younger in age.
WARNING Monitor results of patient’s CBC and other laboratory tests for signs of blood dyscrasias because zonisamide is a sulfonamide and can be absorbed systemically. Systemic absorption may result in life-threatening reactions, including toxic epidermal necrolysis, Stevens-Johnson syndrome, fulminant hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias.

Be aware that patients receiving doses of 300 mg daily or more are at increased risk for adverse CNS reactions, including decreased concentration, fatigue, drowsiness, and impaired speech.

Monitor serum creatinine and BUN levels for signs of abnormally decreased glomerular filtration rate (GFR). Expect some decrease in GFR during first 4 weeks of treatment and return to baseline within 2 to 3 weeks after drug is discontinued.

Monitor patient for signs and symptoms of renal calculi.

Be aware that zonisamide shouldn’t be discontinued abruptly because doing so may increase frequency of seizures.

Monitor patient closely for evidence of suicidal thinking or behavior, especially when therapy starts or dosage changes.

PATIENT SAFTY

Inform patient that zonisamide is usually prescribed with other anticonvulsants and that she should continue to take all as prescribed.

Instruct patient to swallow zonisamide capsules whole and not to chew them or break them open.

Inform patient that prescriber may have to adjust zonisamide dosage over several weeks or months before stable dose is achieved.

Advise patient to use caution when driving or performing other activities that are hazardous or require mental alertness because zonisamide commonly causes somnolence, dizziness, and decreased concentration, particularly during first month of therapy.

Advise patient to wear a medical identification bracelet or necklace or carry medical identification with information about her seizure disorder.

Unless contraindicated, encourage patient to drink 6 to 8 glasses of water each day to prevent kidney stones.

Advise patient to rise slowly from a lying or seated position to reduce the risk of dizziness.

Urge caregivers to watch closely for evidence of suicidal tendencies, especially when therapy starts or dosage changes, and to report concerns immediately to prescriber.

Trade Name & Company Name

Trade name	Company name
METHOTREXATE 2.5MG TAB	EBEWE PHARMA

effect of in Pregnancy, Fetal Health and Breast feeding

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Pindolol is considered a second-line drug (methyldopa, labetolol, or calcium channel blockers are first-line) for the treatment of nonsevere, chronic hypertension during pregnancy. It does not increase uterine contractility. Pindolol is superior to propranolol for the control of 899 preeclamptic hypertension when hydralazine alone is inadequate. Women with preeclampsia treated with pindolol reportedly have a greater decline in Doppler-determined uterine artery flow resistance compared to women treated with propranolol.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Pindolol crosses the human placenta, achieving variable F:M ratios ranging from 0.4 to 4.5 measured at 6h. Doppler flow studies are reassuring with no detectable impact on fetal hemodynamics when given to women with mild preeclampsia. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Pindolol enters human breast milk, achieving variable M:P ratios ranging from 0.5 to 3.5.

Pregnancy

. Pioglitazone improves glycemic control while decreasing circulating insulin and free fatty acid levels and increasing HDL and LDL. When used alone, it is slightly less potent than the sulfonylureas and metformin. Clearance is increased by 20-60% in nonpregnant women compared to men. There is no published experience in pregnancy. It may be useful in the treatment of infertility associated with PCOS.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pioglitazone crosses the human placenta. Rodent studies are for the most part reassuring, revealing no evidence of teratogenicity or functional or behavioral abnormalities despite the use of doses higher than those used clinically. There is evidence of embryotoxicity.

Breastfeeding

There is no published experience with pioglitazone during lactation. It is unknown whether it enters human breast milk. Pioglitazone is excreted into rat breast milk.

Pregnancy

. Piperacillin is widely distributed, including therapeutic levels in bone, heart, bile, and CSF during inflammation. It is best studied during

Pregnancy

for the treatment of gonorrhea, PPROM, and cesarean section prophylaxis. Piperacillin pharmacokinetics reveal a larger volume of distribution and higher clearance rate during pregnancy. This suggests higher doses are necessary for effective treatment of serious infections in pregnant women near term and in the puerperium. In reference to prophylaxis, no single antibiotic proved effective for prophylaxis (ampicillin, cefazolin, cefotetan, piperacillin [? tazobactam]) is superior to the other; cost and convenience are the deciding variables. Piperacillin may be given as a single 4g dose at cord clamping with little loss of efficacy. Several reports support the use of piperacillin (3-4g IV q6h ?72h) to prolong the latency interval between PPROM and the onset of labor.

Fetal Health

There are no adequate reports or well-controlled studies of piperacillin in human fetuses. Placental transfer is rapid, achieving an F:M ratio between 0.25 and 0.3. The concentration in AF is similar to fetal serum. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only small amounts of piperacillin enter human breast milk, and poor oral absorption should limit availability. It is usually considered compatible with breastfeeding. 902

Pregnancy

. Tazobactam is a b-lactamase inhibitor with no significant antibacterial activity; its addition expands the antibacterial spectrum of piperacillin. Piperacillin-tazobactam is active against most strains of the following piperacillin-resistant b-lactamase?producing microorganisms: MSSA, E. coli, H. influenzae (not ampicillin-resistant), and the B. fragilis group (B. fragilis, B. ovatus, B. thetaiotaomicron, or B. vulgatus). The addition of tazobactam does not improve efficacy as a post?cesarean section prophylaxis agent over piperacillin alone. Clearance of the combination appears enhanced during pregnancy. It is similar to ampicillin-gentamicin in efficacy for the treatment of postpartum endometritis.

Fetal Health

There are no adequate reports or well-controlled studies of piperacillin-tazobactam in human fetuses. Placental transfer of tazobactam is rapid, reaching an F:M ratio between 0.25 and 0.3. The concentration in AF is similar to fetal serum. Rodent studies at doses up to 4the MRHD are reassuring, showing no evidence of impaired fertility or teratogenicity. See Piperacillin.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only small amounts of piperacillin enter human breast milk, and poor oral absorption would limit availability. It is not known whether tazobactam enters human breast milk. It is usually considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of piperazine in pregnant women. The long clinical experience is reassuring. Paralysis of the parasite is mediated by its agonist effects upon the inhibitory GABA receptor. Its selectivity for helminths is derived from the fact that vertebrates use GABA only in the CNS and the helminths? GABA receptor is a different isoform.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether piperazine crosses the human placenta.

Breastfeeding

There is no published experience in nursing women. It is unknown whether piperazine enters human breast milk.

Pregnancy

. There is no published experience with pirbuterol in pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies of pirbuterol in human fetuses. Rodent studies, both inhalational and oral, are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Fetal toxicity was noted at the higher doses tested.

Breastfeeding

There is no published experience during lactation. It is unknown whether pirbuterol enters human breast milk.

Pregnancy

. Piroxicam is an orally absorbed oxicam with anti-inflammatory, analgesic, and antipyretic properties. There are no adequate reports or well-controlled studies in pregnant women. In a rodent model, piroxicam decreased the efficacy of IUD-mediated contraception. In one RCT, piroxicam was noted to increase implantation and

Pregnancy

rates after embryo transfer in both fresh and frozen-thawed cycles during IVF. The beneficial effect seemed more pronounced in patients <40y with tubal, or male factor infertility, or endometriosis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Piroxicam presumably crosses the human placenta as do other NSAIDs, and is associated with severe fetal oligohydramnios in case reports. Piroxicam increases the incidence of dystocia and delayed parturition in animals if administered continuously late into pregnancy. Toxic maternal doses are associated with fetal bone demineralization. 907

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only trace quantities of piroxicam are excreted into human breast milk, and do not pose a threat to the Breastfeeding neonate.

Pregnancy

. There is no published experience with plicamycin in pregnancy. It is most commonly used for the treatment of testicular cancer.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether plicamycin crosses the human placenta. Rodent teratogenicity studies apparently have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether plicamycin enters human breast milk. It is unknown whether it alters the constituents of the milk produced.

Pregnancy

. Pneumococcal infection is a leading cause of death and a major cause of pneumonia, meningitis, and otitis media. Pneumococcal vaccine is a mixture of highly purified capsular polysaccharides from the 23 clinically relevant pneumococcal types accounting for at least 90% of pneumococcal blood isolates. The antibody induced by the vaccine may persist for as long as 5 years. Susceptible patients at increased risk include HIV-infected women.

Fetal Health

There are no adequate reports or well-controlled studies of pneumococcal vaccine in human fetuses. Stimulated antibodies are transferred across the placenta. While gestational age affects the efficiency of antibody transfer, vaccination is efficient and newborns of treated women have higher titers during the first 6mo to 1y of life. That said, there is insufficient evidence to conclude maternal pneumococcal vaccination will indeed reduce infant infection. Maternal immunization does not alter the neonatal response to vaccination. Rodent teratogenicity studies have not been performed, though there is no reason to expect an adverse fetal effect. Vaccinated rodents transfer enough antibody to their offspring to protect against otitis media.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether pneumococcal vaccine enters human breast milk. However, the IgA antibody levels for many of the serotypes included are enhanced and may provide enhanced neonatal protection.

Pregnancy

. Podofilox is related to podophyllum resin. There are no adequate reports or well-controlled studies in pregnant women. Toxicity with overuse is reported, but systemic absorption of doses up to 1.5ml is low. Podofilox should not be used to treat large lesions during pregnancy. Though an effective agent, there are other therapies, such as laser and cryotherapy, that pose fewer risks.

Fetal Health

There are no adequate reports or well-controlled studies of podofilox in human fetuses. While many antimitotic drugs are embryotoxic, topical applications of 0.1-1.5ml produce peak serum levels <17ng/ml 1-2h after the application. The elimination t/2 is <4.5h and it does not accumulate after multiple treatments. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level after the treatment of small warts. Limited rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether podofilox enters human breast milk. However, considering the indication and dosing, podofilox use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Podophyllum resin is a mixture of resins from the mandrake (Podophyllum peltatum Linne?), a perennial plant of the northern and middle US. It is made exclusively from American podophyllin, which has a lower level of podophyllotoxin than the n resin. There are no adequate reports or well-controlled studies in pregnant women. Though systemic absorption of doses up to 1.5ml is low, toxicity is reported with overuse. Thus, podophyllum resin should not be used during

Pregnancy

for large lesions. Though an effective agent, there are other therapies, such as laser and cryotherapy, that pose fewer risks.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether podophyllum resin crosses the human placenta. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level after the treatment of small warts. There are reports of complications associated with the topical use of podophyllin on condylomata of pregnant patients, including birth defects, fetal death, and stillbirth. The relationship of outcome to the use of podophyllum resin is unclear.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether podophyllum resin enters human breast milk. However, considering the indications and dosing, podophyllum resin use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Inactivated poliovirus vaccine is a sterile suspension of three types [type 1 (Mahoney), type 2 (MEF-1), and type 3 (Saukett)] grown in culture and inactivated with formaldehyde. Neomycin, streptomycin, and polymyxin B are each used in vaccine production. Paralytic poliomyelitis has not been reported after vaccination. Routine primary poliovirus vaccination of adults (>18y) living in the US is not recommended. Adults at increased risk of exposure but not previously immunized should be vaccinated. This group includes travelers to regions where poliomyelitis is endemic or epidemic, health care workers in close contact with patients who may be excreting polioviruses, laboratory workers handling specimens that may contain polioviruses, members of groups with disease caused by wild polioviruses, and incompletely vaccinated or unvaccinated adults in contact with children given live oral poliovirus vaccine. Vaccination during

Pregnancy

is effective, and the antibodies are detectable in the fetus.

Fetal Health

There are no adequate reports or well-controlled studies of inactivated poliovirus vaccine in human fetuses. Poliovirus antibodies cross the human placenta and may offer some perinatal protection. Rodent teratogenicity studies have not been conducted, though an inactivated virus should not pose a significant fetal risk.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. While it is unknown whether inactivated poliovirus vaccine enters human breast milk, the resulting antibodies might. However, it appears the oral vaccine is superior for the stimulation of IgA.

Pregnancy

. Oral poliovirus vaccine is a live, trivalent mixture of three types of attenuated polioviruses grown in monkey kidney cell culture. Oral poliovirus vaccine simulates natural infection, inducing active mucosal and systemic immunity without producing symptoms of disease. Routine primary poliovirus vaccination of adults (>18y) living in the US is not recommended. Adults who are at increased risk of exposure and who have not been adequately immunized should receive poliovirus vaccination. This group includes travelers to regions where poliomyelitis is endemic or epidemic, health care workers in close contact with patients who may be excreting polioviruses, laboratory workers handling specimens that may contain polioviruses, and members of groups with disease caused by wild polioviruses. Oral poliovirus vaccine is used for epidemic control. Vaccination during

Pregnancy

is effective and does not increase the risk of a

Pregnancy

complication.

Fetal Health

There are no adequate reports or well-controlled studies of oral poliovirus vaccine in human fetuses. Maternal vaccination results in a level of passive immunity for the newborn. There is no evidence of teratogenicity or fetal toxicity. Rodent teratogenicity studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Antibodies are found in breast milk. While it is unknown whether oral poliovirus vaccine enters human breast milk, the resulting IgA antibodies do and may offer a level of neonatal protection. It is generally considered compatible with breastfeeding.

Pregnancy

. There is little if any systemic absorption of polyethylene glycol. There are no adequate reports or well-controlled studies in pregnant women. It is used successfully for the treatment of puerperal constipation.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether polyethylene glycol crosses the human placenta. However, it is unlikely a clinically significant quantity is absorbed systemically. Rodent teratogenicity studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether polyethylene glycol enters human breast milk. Considering the lack of systemic absorption, polyethylene glycol is unlikely to achieve clinically relevant levels in breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of polymyxin B?trimethoprim in pregnant women. (See Trimethoprim.)

Fetal Health

There are no adequate reports or well-controlled studies of polymyxin B?trimethoprim in human fetuses. Considering the dose and route, it is unlikely the maternal systemic concentrations will reach clinically relevant levels. (See Trimethoprim.)

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether polymyxin B?trimethoprim enters human breast milk. However, considering the indication, route, and dosing, polymyxin B?trimethoprim use is unlikely to pose a clinically significant risk to the

Pregnancy

. There are no adequate reports or well-controlled studies of polythiazide-prazosin in pregnant women. (See Prazosin.)

Fetal Health

There are no adequate reports or well-controlled studies of polythiazide-prazosin in human fetuses. (See Prazosin.) 916

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether polythiazide-prazosin enters human breast milk. (See Prazosin.)

Pregnancy

. There are no adequate reports or well-controlled studies of potassium chloride in pregnant women. The most common cause of hypokalemia during

Pregnancy

is the administration of b-mimetic agents for the treatment of preterm labor (see Ritodrine, Terbutaline). However, the decreased serum potassium does not reflect total body depletion, but rather increased intracellular potassium. Routine treatment is not necessary. 917

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Potassium chloride readily crosses the human placenta. It is unlikely that potassium supplementation would have an adverse effect on the fetus without maternal toxicity. Rodent reproduction studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Potassium chloride enters human breast milk; supplementation is generally considered compatible with breastfeeding.

Pregnancy

. Potassium iodide effectively reduces thyroid uptake of radioactive iodide and is an adjunct for women with hyperthyroidism associated with Graves? disease. There are no adequate reports or well-controlled studies in pregnant women. Potassium iodide replacement is effective during

Pregnancy

for the treatment of mild to moderate iodine deficiency.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Potassium iodide crosses the human placenta, 918 and an excess can cause fetal goiter and hypothyroidism. The limited rodent studies are reassuring.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Supplementation with potassium iodide has little effect on the iodine concentration of human breast milk. It is probably compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of pralidoxime in pregnant women. The published experience is limited to case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is not known whether pralidoxime crosses the human placenta. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There is no published experience in nursing women. It is unknown whether pralidoxime enters human breast milk. 919 However, considering the indication and dosing, one-time pralidoxime use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Pramipexole clearance is 30% lower in women than men; most of this difference reflects body weight. The published experience during

Pregnancy

is limited to two case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pramipexole crosses the human placenta. Pramipexole in rodents reduces implantation and is embryotoxic. Teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether pramipexole enters human breast milk. Pramipexole is concentrated in rodent milk.

Pregnancy

. Pravastatin lowers lipids in two ways. First, it modestly reduces the intracellular pool of cholesterol by the reversible inhibition of HMG-CoA reductase, increasing the number of LDL receptors on cell surfaces and enhancing receptor-mediated catabolism and clearance of circulating LDL. Second, pravastatin inhibits LDL production by inhibiting hepatic synthesis of VLDL, the LDL precursor. There are no adequate reports or well-controlled studies in pregnant women. Atherosclerosis is a chronic process; discontinuation of pravastatin during

Pregnancy

should have little impact on long-term maternal outcome.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pravastatin crosses the 921 human placenta. It is lipophilic and should equilibrate between maternal and fetal compartments. Pravastatin inhibits P-glycoprotein and therefore may increase the placental transfer of other compounds to the fetus. One recent review of 214

Pregnancy

exposures to statins noted 31 adverse outcomes, including 22 cases with structural defects and 5 fetal deaths. There were two principal categories of recurrent structural defects: cerivastatin and lovastatin were associated with 4 reports of severe midline CNS defects; simvastatin, lovastatin, and atorvastatin were associated with reports of limb deficiencies, including 2 similar complex lower limb defects after simvastatin exposure. There were 2 cases of VACTERL among the limb deficiency cases. No adverse outcomes were reported after exposure to pravastatin, which is poorly transported across the rodent placenta. These authors concluded that statins may have secondary effects on sterol-dependent morphogens such as Sonic Hedgehog.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether pravastatin enters human breast milk. Certainly cholesterol and its by-products are important components of breast milk. In the absence of further study, pravastatin should be considered incompatible with breastfeeding.

Pregnancy

. Schistosomiasis affects approximately 40 million women of childbearing age, yet little is known about schistosome-associated morbidity in pregnant women and their offspring. The WHO has recommended treatment of infected pregnant and lactating women. The main complication of helminth infection during

Pregnancy

is anemia. Neurocysticercosis is a cause of first-time convulsions in pregnant patients, and there are several case reports of its successful treatment with praziquantel during pregnancy. Praziquantel has also been used during the puerperium to successfully treat hypersplenism secondary to chronic hepatosplenic schistosomiasis. Recent study documents that

Pregnancy

suppresses a potentially beneficial boost in cytokine responses associated with praziquantel.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is not known whether praziquantel crosses the human placenta. Congenital helminthic infection in humans is exceedingly rare. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. However, some studies report praziquantel is embryotoxic and may be genotoxic.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Praziquantel enters human breast milk with an M:P ratio approximating 0.25 or a peak milk concentration of 0.5mg/ml. However, the mean excretion with the milk in 24h approximates 0.0008% of the given dose. Thus, the unsupplemented neonate of a woman treated for tapeworm would ingest less than 1mg of drug given to its mother.

Pregnancy

. Unlike many other antihypertensive drugs, the effect of prazosin is closely related to its plasma concentration. The Tmaxis increased and its elimination t/2 prolonged during pregnancy. Prazosin is a secondary agent for the treatment of preeclamptic hypertension. While as effective as nifedipine, the associated fetal death rate is higher. Prazosin has revolutionized the treatment of severe scorpion stings.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Prazosin crosses the human placenta, achieving an F:M ratio of 0.20. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Some decrease in litter size occurs at doses >200the MRHD. There is no apparent explanation for the increased perinatal mortality rate when used to treat preeclamptic hypertension.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Small quantities of prazosin enter human breast milk; however, it is generally considered compatible with breastfeeding.

Pregnancy

. Prednicarbate (0.1%) does not suppress the HPA-axis if used at 30g/d for 1w. There are no published studies in pregnant women.

Fetal Health

There are no published studies in human fetuses. It is unknown whether prednicarbate crosses the human placenta. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level. In some rodent studies, prednicarbate is teratogenic and embryotoxic if given SC at doses 45the recommended topical human dose, assuming a percutaneous absorption of approximately 3%.

Breastfeeding

There is no published experience in nursing women. It is unknown whether prednicarbate enters human breast milk. Some systemically administered corticosteroids are excreted in breast milk. However, considering the route and concentration, limited prednicarbate use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Prednisolone is a metabolite of prednisone. It provides effective relief (10mg PO tid) of severe hyperemesis unresponsive to primary therapy and characterized by at least a 10% weight loss. Dermatologic and ophthalmic applications have been used for decades during

Pregnancy

without apparent sequelae. Prednisolone is used widely for the treatment of inflammatory/ autoimmune disorders that are common in reproductive-age women. Once used for the treatment antiphospholipid syndrome, several trials document a higher loss rate with prednisolone and aspirin than heparin and aspirin. Similarly, the combination of prednisone, aspirin, and progesterone is no better than enoxaparin alone for the treatment of idiopathic, recurrent miscarriage.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. The human placenta metabolizes prednisone, reducing fetal exposure to perhaps 10% of the maternal level. 926 One study of prenisolone placental transfer noted the same F:M of 0.10. Prednisone is often used as salvage therapy for the treatment of fetal alloimmune thrombocytopenia in fetuses unresponsive to immune globulin infusion. Some authors suggest emotional stress during organogenesis could cause congenital malformations by increasing the level of glucocorticoids. Older epidemiologic studies examined the association of oral clefting with corticosteroids exposure and concluded prenatal exposure carried 6-fold increase in risk for cleft lip with or without cleft palate. IUGR and shortening of the head and mandible were also suggested as sequelae. However, the Collaborative Perinatal Project followed women treated during the 1st trimester. While the number of exposures was limited, no increase in congenital malformations was detected. More recent studies also dismiss the risk of teratogenicity for all malformations except clefting. There is no increase in risk of anomalies when exposure occurs after organogenesis. Women exposed to topical prednisone-like compounds during

Pregnancy

have no significantly increased risk of delivering a child with birth defects. In sum, the evidence that corticosteroids are human teratogens is weak, and confined only to cleft lip. Female rats exposed to cortisone in utero exhibit premature vaginal opening. Cortisone accelerates fetal rat intestinal maturation, perhaps explaining why corticosteroids decrease the incidence of NEC.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether prednisolone enters human breast milk. However, long clinical experience suggests prednisolone therapy is compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of prednisone in pregnant women. Crohn?s disease and other chronic inflammatory diseases often affect reproductive-age women. The available data show that women with Crohn?s disease can expect to conceive successfully, carry to term, and deliver a healthy baby. Control of disease activity before conception and during

Pregnancy

is critical to optimize both maternal and fetal health. The pharmacologic therapy during

Pregnancy

is similar to that for nonpregnant patients. Patients maintained in remission by way of pharmacologic therapy should continue it throughout their pregnancy. Although prednisolone was previously used for the treatment antiphospholipid syndrome, several trials report the loss rate is higher with prednisolone and aspirin versus heparin and aspirin. Though there are several case series suggesting prednisone is of benefit, there is insufficient evidence to determine whether adjunctive steroid use in HELLP syndrome decreases maternal and perinatal mortality or major maternal and perinatal morbidity.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. The human placenta metabolizes prednisone, reducing fetal exposure to perhaps 10% of the maternal level. Some authors suggest emotional stress during organogenesis could cause congenital malformations by increasing the level of glucocorticoids. Prednisone is used as a rescue therapy for the treatment of fetal alloimmune thrombocytopenia when IVIG has failed. Older epidemiologic studies examined the association of oral clefting with corticosteroids exposure and concluded prenatal exposure carry a 6- fold increase in risk for cleft lip with or without cleft palate. IUGR and shortening of the head and mandible were also suggested as sequelae. However, the Collaborative Perinatal Project followed women treated during the 1st trimester. While the number of exposures was limited, no increase in congenital malformations was detected. More recent studies also dismiss the risk of teratogenicity for all malformations except clefting. There is no increase in risk of anomalies when exposure occurs after organogenesis. Women exposed to topical prednisone-like compounds during

Pregnancy

have no significantly increased risk of delivering a child with birth defects. In sum, the evidence that corticosteroids are human teratogens is weak, and confined only to cleft lip. Female rats exposed to cortisone in utero exhibit premature vaginal opening. Cortisone accelerates fetal rat intestinal maturation, perhaps explaining why corticosteroids decrease the incidence of NEC.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether prednisone enters human breast milk. However, most asthma medications, including oral prednisone, are considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Prilocaine is used in some locales for pudendal nerve block at delivery. Prilocaine causes vascular smooth muscle contraction in in vitro studies, suggesting injection in the region of the uterine artery for a paracervical block may be a risk. Prilocaine is also available solid as a cream with lidocaine. In one RCT, lidocaine-prilocaine cream did not decrease the discomfort associated with amniocentesis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Prilocaine crosses the human placenta, and after pudendal nerve block achieves an F:M ratio near unity. There are several reports of neonatal methemoglobinemia after prilocaine. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether prilocaine enters human breast milk. However, considering the indication and dosing, one-time prilocaine use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Primaquine is mainly used to treat the P. vivax or P. ovale malaria. Once the parasite has been eliminated from the bloodstream, the remaining hypnozoites must be removed from the liver by administering a 14d course of primaquine (the so-called radical cure). Primaquine is considered by some to be contraindicated in

Pregnancy

since the G6PD status of the fetus will be unknown. A pregnant woman should take weekly chloroquine prophylaxis until after delivery when hypnozoite eradication can be initiated. Primaquine is not routinely used to prevent malaria in travelers, and as such is only used when no other alternatives exist. It is not licensed for this use in the US or UK. Primaquine causes methemoglobinemia in all patients (levels of up to 18% are reported, normal level <1%), but this seldom causes symptoms and is always self-limiting. Dangerous levels of methemoglobinemia only occur in patients with G6PD deficiency.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Primaquine likely crosses the human placenta, as it may be associated with a hemolytic crisis in a G6PD-deficient fetus. Except for the tetracyclines, there is no evidence that at recommended doses any of the antimalarial drugs are teratogenic. Primaquine is generally not recommended because of its theoretic potential to cause fetal hemolytic anemia. Rodent teratogenicity studies apparently have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether primaquine enters human breast milk.

Pregnancy

. Primidone is metabolized to phenobarbital and PEMA. PEMA potentiates the effect of phenobarbital. There are no adequate reports or well-controlled studies in pregnant women, though levels reportedly decline with advancing gestation. Primidone is used mainly to treat complex partial, simple partial, generalized tonic-clonic, myoclonic, and akinetic seizures. It has been a valuable alternative to propranolol for the treatment of essential tremor. Unlike other AEDs such as carbamazepine and valproic acid, primidone is rarely used in the treatment of bipolar disorder or any other psychiatric problem. It has occasionally been used to treat long QT syndrome, cerebral palsy, and athetosis. AEDs should not be discontinued in patients to whom they are given to prevent major seizures because of the strong possibility of precipitating status epilepticus with attendant hypoxia and threat to life. In individual cases where the severity and frequency of the seizure disorder are such that the removal of medication does not pose a serious threat to the patient, discontinuation of the drug may be considered prior to and during pregnancy, although it cannot be said with any confidence that even minor seizures do not pose some hazard to the developing embryo or fetus.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Phenobarbital and PEMA readily crosses the human placenta, and are distributed throughout fetus. The highest concentrations are found in the placenta and fetal liver and brain. Withdrawal symptoms may occur in infants exposed to barbiturates throughout the 3rd trimester. Reports suggesting an increased rate of birth defects (oral clefting and cardiac malformations) in children of drug-treated epileptic women are not adequate to prove a cause-and-effect relationship, but there does appear to be a clear increased risk of neurologic dysfunction. The likelihood of congenital abnormalities in children exposed in utero to carbamazepine, phenobarbital, phenytoin, and primidone is reduced but not eliminated by folic acid supplementation 5-12w from LMP. The majority of mothers on anticonvulsant medication deliver normal infants. Anticonvulsant drugs should not be discontinued in patients in whom the drug is administered to prevent major seizures because of the strong possibility of precipitating status epilepticus with attendant hypoxia and threat to life. As for most psychotropic drugs, monotherapy and the lowest effective quantity given in divided doses to minimize the peaks can minimize the fetal risks. It is controversial whether enzyme-inducing drugs such as primidone increase the risk of neonatal bleeding. Though the most recent studies indicate not, the administration of 1mg vitamin K IM at birth is common. 933

Breastfeeding

There is no published experience in nursing women. Primidone and its metabolites are excreted into human breast milk and have been associated with neonatal sedation. If Breastfeeding continues, the infant should be monitored for possible adverse effects, the drug given at the lowest effective dose, and

Pregnancy

. Probenecid is used during

Pregnancy

with a penicillin almost exclusively for the treatment of STDs. 934

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Probenecid crosses the human placenta, but is not associated with adverse fetal effects. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Experience is limited to a single informative case report. A breastfed infant of a 30y-old woman being treated with probenecid and cephalexin for a breast infection developed severe diarrhea and associated symptoms. Milk was collected over a dose interval at steady-state, and concentrations of probenecid and cephalexin measured by HPLC. The average concentrations of probenecid and cephalexin in the milk were 964 and 745mcg/L, respectively, corresponding to absolute and relative infant doses of 145mcg/kg/d and 0.7% for probenecid and 112mcg/kg/d and 0.5% for cephalexin. Neither drug level is such that an effect would be expected. Considering the indication and dosing, the typically one-time use of probenecid is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Probucol is not marketed in the US. There is no published experience with probucol during pregnancy. Atherosclerosis is a chronic process; discontinuation of probucol during

Pregnancy

should have little impact on the long-term outcome of the disease process.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether probucol crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether probucol enters human breast milk. Certainly cholesterol and its by-products are important components of breast milk. In the absence of further study, probucol should be considered incompatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Procainamide is well tolerated, and is a first-line agent for the treatment of acute, undiagnosed, wide-complex tachycardia. It may be used alone or in combination with digoxin. All class IA agents should be administered in the hospital under continuous cardiac monitoring due to the potential risk of ventricular arrhythmia. Electrical cardioversion is necessary in all patients who are hemodynamically unstable with life-threatening ventricular tachyarrhythmias. In hemodynamically stable patients, initial therapy with ajmaline, procainamide, or lidocaine is indicated.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Procainamide crosses the human placenta and is not bound by the placenta. There are numerous case reports of its use as a transplacental agent to treat fetal arrhythmia. In vitro, it produces dose-dependent relaxation of the placental vasculature. Rodent teratogenicity studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Both procainamide and its main metabolite, NAPA, are excreted into human breast milk and absorbed by the nursing neonate. Yet, the circulating level achieved is low and procainamide is considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Procaine has been used for decades during labor to create spinal, nerve block, or infiltration anesthesia.

Fetal Health

There are no adequate reports or well-controlled studies of procaine in human fetuses. Local anesthetics rapidly cross the placenta. The long clinical experience is reassuring. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether procaine enters human breast milk. However, considering 938 the indication and dosing, one-time procaine use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Procarbazine is usually combined with other potent antineoplastic agents. Yet the outcomes for most treated pregnancies and the 2nd-generation children are normal.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. While it is unknown whether procarbazine crosses the human placenta, there are case reports of malformations in the offspring of women exposed to procarbazine in combination with other antineoplastic agents. Rodent studies performed at multiples of the MRHD reveal a spectrum of malformations, including a dose-dependent increase in microcephaly and cleft lip/palate. Supplementation with folate reduces the prevalence with a gender-specific effect (M>F).

Breastfeeding

There is no published experience in nursing women. It is unknown whether procarbazine enters human breast milk. 939

Pregnancy

. Prochlorperazine is most often used for the short-time treatment of N/V and vertigo. There are no adequate reports or well- controlled studies in pregnant women. In the UK, prochlorperazine is available OTC as Buccastem M in buccal form for the treatment of migraine. In this indication it blocks the chemoreceptor trigger zone in the brain that is responsible for causing severe N/V. Its OTC use is restricted to a maximum of 2d because of the potentially severe Side effects include agranulocytosis, thrombocytopenia, hemolytic anemia, ECG abnormalities, exfoliative dermatitis, tardive 940 dyskinesia, neuroleptic malignant syndrome, hepatotoxicity, leukopenia, drowsiness, amenorrhea, blurred vision, rash, orthostatic hypotension, jaundice, dry mouth, constipation, photosensitivity, anxiety, oculogyric crisis, and extrapyramidal effects.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether prochlorperazine crosses the human placenta. The extensive clinical experience during

Pregnancy

is reassuring, without any substantial evidence of teratogenicity. Rodent teratogenicity studies have not been performed. Breastfeeding There are no adequate reports or well-controlled studies in nursing women. Prochlorperazine enters human breast milk, but the kinetics remain to be elucidated.

Pregnancy

. There is no published experience with procyclidine in pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether procyclidine crosses the human placenta. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether procyclidine enters human breast milk.

Pregnancy

. Progesterone is central for reproduction. This section applies only to native hormone and not synthetic compounds, which may differ significantly depending upon their receptor profile (see individual progestogens). Progesterone is used throughout the 1st trimester to provide luteal-phase support for women undergoing ovulation induction and IVF. Other than those, there are no proved indications for its use during pregnancy. Progesterone administration does not prevent

Pregnancy

loss in women with spontaneous, clinically recognized conceptions greater than 7w when the placenta is hormonally functional and the

Pregnancy

no longer corpus luteum dependent. The evidence that progesterone is an effective treatment for supposed luteal-phase defects is weak. Recent study suggests the administration of micronized progesterone vaginal gel or cream to women with a sonographically short cervix (10-15mm) between 22 and 24w gestation is associated with a 40% reduction in the incidence of idiopathic preterm birth. While the MFMU Network trial also concluded 17-hydroxy progesterone caproate administered weekly IM had a similar efficacy in women with at least one prior 942 idiopathic preterm birth, a more recent investigation mounted to obtain FDA approval for the vaginal gel failed to reproduce this conclusion. However, in a secondary analysis, these investigators did find a significant reduction in the incidence of idiopathic preterm birth when treated subjects had a sonographic cervical length at randomization <28mm. This finding is consistent with the finding that pregnant women with a prior idiopathic preterm birth but a normal sonographic cervical length in the current gestation are not at increased risk for recurrent idiopathic preterm birth.

Fetal Health

There are no adequate reports or well-controlled studies of progesterone in human fetuses. Progestogens differ in their hormonal effects. Masculinization of the female fetus is attributed to some progestogens. The evidence that natural progesterone is a teratogen is weak.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Exogenous progesterone enters human breast milk. The quantity of milk produced correlates with the antenatal progesterone level.

Pregnancy

. Promazine is a prototype phenothiazine used with variable success for the treatment of depressive neurosis, alcohol withdrawal, N/V, symptoms of dementia, Tourette?s syndrome, Huntington?s chorea, and Reye?s syndrome. An older medication used to treat schizophrenia, its use has largely been replaced by newer agents such as olanzapine and quetiapine. Though promazine has been used in obstetrics for almost 3 decades, there are no adequate reports or well-controlled studies in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether promazine crosses the human placenta. However, it undergoes placental peroxidation, and the free radicals produced may be one source of fetal toxicity. Older reports suggest a relationship between antenatal promazine and neonatal hyperbilirubinemia. In one study, promazine had no effect on fetal CV function of sheep. In a second study performed using a higher dose, promazine caused fetal hypotension and tachycardia, and exacerbated the effect of umbilical cord compression. Rodent teratogenicity studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether promazine enters human breast milk.

Pregnancy

. Promethazine has been used for decades in obstetrics to treat N/V, as a sedative, and to relieve apprehension during the latent phase of labor. It is often combined with a narcotic such as meperidine. Promethazine (25mg tid ?3w) is similar to ondansetron but inferior to a short course (3d) of methylprednisolone for the relief of N/V of pregnancy. Promethazine was a frequent component of lytic cocktails used in preeclamptic women to prevent seizures. These cocktails have been abandoned in favor of magnesium sulfate. Initial hopes that promethazine would ameliorate severe Rh alloimmunization have not been substantiated but remain poorly studied. It is not effective for the relief of nausea following thiopentone anesthesia for abortion. Controlled trials do not support the use of promethazine as an adjuvant to reduce postoperative adhesions. It has been used unsuccessfully for the relief of postepidural pruritus associated with morphine injection.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether promethazine crosses the human placenta. Human epidemiologic studies are reassuring. The combination of promethazine and meperidine during labor reduces FHR reactivity. There was no effect on somatic 945 development in one study. Transport across the mouse placenta is limited. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. A recent epidemiological study found no adverse outcomes after an attempted suicide with promethazine.

Breastfeeding

There is no published experience in nursing women. It is unknown whether promethazine enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of propafenone in pregnant women. The published experience is confined to case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Propafenone crosses the human placenta, though the kinetics remain to be elucidated. Rodent studies reveal embryotoxicity but no evidence of teratogenicity. Embryotoxicity occurs increasingly with escalating doses.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Limited study suggests low quantities of propafenone enter human breast milk, with an M:P ratio of 0.25 and a theoretic infant dose of 0.1% of the daily maternal dose.

Pregnancy

. There is no published experience with propantheline in pregnancy. 948

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether propantheline crosses the human placenta. Rodent teratogenicity studies apparently have not been performed.

Breastfeeding

There is no published experience during lactation. It is unknown whether propantheline enters human breast milk.

Pregnancy

. Propofol is popular for a variety of procedures including oocyte retrieval and suction curettage. Its administration (1.0mg/kg/h) after cord clamping at cesarean delivery performed under general anesthesia reduces postoperative N/V. In addition, an IV bolus (20mg) decreases pruritus associated with intrathecal morphine. Its clearance, as reflected in the dose required to produce unconsciousness, is unaltered during early pregnancy. It has a direct inhibitory effect on uterine contractions, caused at least in part by interfering with calcium transport. In small series of patients whose anesthesia for cesarean delivery was induced and maintained with propofol, there were no differences in neonatal outcome as compared to more commonly administered anesthetic agents.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Propofol crosses the human placenta in a time-dependent manner, at a rate dependent on uterine and umbilical blood flows. The maternal albumin level also impacts on the extent of transfer. Reports of F:M ratio range widely from 0.35 to 1.0. Propofol infusions adequate for conscious sedation during cesarean section seem to have no adverse neonatal effects. In the ewe, a 6mg/kg IV bolus followed by a continuous infusion of 0.4mg/kg/min produced an AUC and Cmaxof 8.6 mg/h/ml and 9.5mg/ml, respectively, higher than those of the fetus (1.6mg/h/ml and 1.19 mg/ml, respectively). The mean t/2 was 0.5h in the ewe and 1.1h in the fetus, suggesting accumulation may occur. While rodent studies are reassuring, revealing no evidence of teratogenicity, breastfed pups of treated mothers have a higher mortality rate. Propofol transiently blocks NMDA receptors that lead to an increase in neuronal apoptosis in rodents.

Breastfeeding

A small amount of propofol is excreted in human breast milk. However, considering the indications, prior exposure to propofol is not likely to pose a significant risk to the Breastfeeding neonate.

Pregnancy

. Propoxyphene is a narcotic, and its combination with other CNS depressants such as alcohol has an additive effect. There are no adequate reports or well-controlled studies in pregnant women. Propoxyphene combinations offer no clinical advantage over NSAIDs for the treatment of episiotomy pain.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Both propoxyphene and its principal active metabolite, norporpoxyphene, cross the human placenta, and and achieve an M:F ratio of unity within 1h. Neonatal addiction/ withdrawal occur. Though there are scattered case reports of miscellaneous birth defects, no pattern has emerged.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. While low levels of propoxyphene are excreted into human breast milk, its use as directed is generally considered compatible with breastfeeding.

Pregnancy

. Propranolol is used extensively during

Pregnancy

for the treatment of maternal hypertension, arrhythmia, and migraine headache, and is generally considered safe. It is also used acutely to provide relief of symptoms from thyrotoxicosis and pheochromocytoma. Several studies suggest the administration of 952 propranolol (2mg IV) to nulliparas who require oxytocin augmentation for dysfunctional labor reduces the likelihood of a cesarean delivery by almost1=2. The studies of propranolol as an oral hypotensive are small. It appears as effective as a- methyldopa, and is often coupled with other hypotensive agents such as hydralazine.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Propranolol crosses the human placenta, but has no effect on either uterine or umbilical Doppler-determined resistances in chronically hypertensive women. There are case reports of its use, usually with digoxin, for the treatment of SVT, though there are superior agents. The impact of propranolol on the fetus of women with chronic hypertension is unclear. Frequently combined with another agent, the risk of IUGR is reportedly increased. However, IUGR is more common when the maternal pressure is suboptimally controlled and in need of higher doses. The most recent information suggests the increased risk of IUGR reflects excessive maternal b blockade adequate to decrease maternal cardiac output. Other neonatal sequelae reported include bradycardia and hypoglycemia.

Breastfeeding

Less than 1% of the maternal dose of propranolol enters human breast milk; it should not pose a risk to the breastfed neonate.

Pregnancy

. Hyperthyroidism occurs in approximately 1 in every 1000-2000 pregnancies. Propylthiouracil historically was the agent of choice for the treatment of Graves? disease during

Pregnancy

because it was believed to have less potential for fetal/neonatal hypothyrodism, to cross the placenta, or to enter breast milk, and to be less teratogenic than methimazole or carbimazole. None of these reasons has been validated in recent studies. There are no 954 adequate reports or well-controlled studies in pregnant women. Methimazole is equally effective. It is generally recommended that the minimum dose of propylthiouracil necessary to control the maternal thyroid be used. However, this is a poor approach as the maternal dosage correlates poorly with the newborn TSH. Clearly, dosing must be individualized to achieve optimal maternal and fetal outcome. Women with a history of Graves? disease in the past should be screened for the continued presence of thyroid-stimulating immunoglobulin even if they previously received definitive treatment, since fetal hyperthyroidism is still likely when positive. Fetal treatment may be necessary, and the patient should be appropriately evaluated in a fetal care unit.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Propylthiouracil crosses the human placenta. The fetuses of mothers treated with propylthiouracil are rarely euthyroid, and a fetal evaluation is mandatory. Hydrops fetalis has been reported as a rare complication of fetal hypothyroidism. Aplasia cutis is a rare complication of maternal therapy. Compromised neurodevelopment in the rodent reflects decreased T4.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Small quantities of propylthiouracil are excreted into human breast milk, but thyroid function of breastfed neonates is unaffected.

Pregnancy

. There are no adequate reports or well-controlled studies of protamine in pregnant women. Case reports note acute hypotension, bradycardia, and anaphylactic reactions. Protamine does not reverse anticoagulation secondary to the LMWHs.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether protamine crosses the human placenta. Rodent teratogenicity studies have not been conducted. However, insulin coupled to protamine has a long safety record.

Breastfeeding

There is no published experience in nursing women. It is unknown whether protamine enters human breast milk. However, insulin coupled to protamine has a long safety record.

Pregnancy

. There are no published reports of protriptyline use in pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether protriptyline crosses the human placenta. There is no evidence after 5y that either TCAs or fluoxetine adversely affect cognition and language development. In contrast, maternal depression is associated with lower language and cognitive achievement. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no published reports in nursing women. It is unknown whether protriptyline enters human breast milk.

Pregnancy

. Pseudoephedrine is second-line therapy behind 1st- and 2nd-generation antihistamines. There are no adequate reports or well-controlled studies in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. The chemical structure of pseudoephedrine suggests it crosses the human placenta. Epidemiologic study suggests exposed fetuses are at increased risk of gastroschisis by as much as 4-fold and, to a lesser degree, small intestinal atresias. The risk may be enhanced by tobacco use. There is a single case report suggesting a relationship with fetal tachycardia. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Less than 1% of the maternal dose of pseudoephedrine is excreted into human breast milk. Though generally considered compatible with breastfeeding, a recent study suggests a single 60mg dose of pseudoephedrine reduces milk volume by 25%. Thus, women with low milk production should 958 consider another decongestant. In this same study, neonatal ingestion was quantified as the product of average steady-state drug concentration in milk, with an estimated milk production rate of 0.15L/kg/d, and expressed relative to the maternal weight-adjusted dose. Assuming maternal dose of 60mg pseudoephedrine PO qid, the estimated infant dose was <5% of the weight-adjusted maternal dose.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Psyllium is not absorbed systemically.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Psyllium is not absorbed systemically and poses no direct threat to the fetus. 959

Breastfeeding

There is no published experience in nursing women. As psyllium is not absorbed systemically, it is unlikely to be excreted into human breast milk.

Pregnancy

. There are no published reports of pyrantel pamoate use in pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pyrantel pamoate crosses the human placenta. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There is no published experience in nursing women. It is unknown whether pyrantel pamoate enters human breast milk.

Pregnancy

. Pyrazinamide should only be given with other antituberculosis agents. It has an excellent safety record during pregnancy. However, there are no adequate reports or well-controlled studies in pregnant women. Most publications consist of case reports or limited series.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pyrazinamide crosses the human placenta. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. In one woman taking 1g pyrazinamide PO, the maternal plasma level 3h later was 1.5mg/L with a theoretic infant daily dose of 0.2mg/kg/d.

Pregnancy

. There are no adequate reports or well-controlled studies of pyridostigmine in pregnant women. The published literature consists of small series and case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pyridostigmine crosses the human placenta. Several case reports suggest a relationship between pyridostigmine and neurologic abnormalities, including arthrogryposis multiplex and microcephaly. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Pyridostigmine is excreted into human breast milk at low concentration (5-25mcg/L). In light of the poor oral absorption, the estimated daily intake would be <0.5% of the maternal dose.

Pregnancy

. Pyridoxine is a coenzyme for several amino acid decarboxylases and transaminases. It reduces N/V of pregnancy, but does not reduce the Side effects include numbness, unsteady gait, and paresthesias.

Fetal Health

Pyridoxine crosses the human placenta and is not teratogenic. Pyridoxine supplementation during

Pregnancy

increases neonatal stores in a dose-dependent manner. Breastfeeding Pyridoxine requirements are thought to increase during lactation. Maternal supplementation increases human breast milk content in a dose-dependent manner.

Pregnancy

. Severe anemia is a cause of maternal morbidity in endemic areas, and treatment leads to resolution. HIV infection during

Pregnancy

is associated with an increased risk of malaria. Pyrimethamine has a long history of use during pregnancy, especially for the treatment of primary toxoplasmosis and malaria. Recent study suggests the use of intermittent preventative therapy in endemic areas.

Fetal Health

Pyrimethamine crosses the human placenta with about 30% efficiency. While it has been long used for the treatment of toxoplasmosis during pregnancy, several recent studies conclude that antenatal therapy does not alter outcome, perhaps because fetal infection has already occurred. Other studies suggest pyrimethamine does not reduce transmission, but rather the sequelae of infection. Further research is required to define the role of prenatal screening and therapy. In contrast, the treatment 964 of pregnant women (in combination with sulfadoxine) in malaria-endemic areas is cost-effective, reducing the risk of prematurity and IUGR secondary to placental malaria. In rodents, pyrimethamine is associated with embryotoxicity and IUGR. Pyrimethamine was associated with an increased risk of cleft palate, micrognathia, and clubfoot in pigs.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Pyrimethamine is excreted into human breast milk in low concentrations. It is estimated the breastfed neonate would ingest less than 10% of the maternal dose over 48h.

Pregnancy

. Quetiapine is a dibenzothiazepine derivative. The published experience during

Pregnancy

is limited to case reports. A single case report suggests the t/2 is decreased by 25-30% throughout

Pregnancy

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Quetiapine crosses the human placenta, achieving an F:M ratio of about 0.25. Only about 4% of the maternal dose is transferred across the isolated cotyledon. The

Pregnancy

outcomes of women who contacted a teratogen information service after exposure to quetiapine appeared normal. Rodent studies are mostly reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. Embryotoxicity and IUGR were noted at the highest doses.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Small amounts of quetiapine are excreted into human breast milk (but in one series only 50% of women had detectable levels in their milk). Detailed kinetics studies are scarce. In one report, the average milk concentration was 41mcg/ L, the M:P ratio (measured using the average concentrations during the elimination phase) was 0.29, and the relative infant dose was 0.09% of the maternal weight-adjusted dose (7273mcg/ kg/d). The infant plasma concentration of 1.4mcg/L was some 6% of the corresponding maternal plasma concentration. No adverse effects were noted in the infant.

Pregnancy

. There are no adequate reports or well-controlled studies of quinapril in pregnant women. In general, ACEIs should be avoided during pregnancy. The lowest effective dose should be used when quinapril is required for BP control during pregnancy.

Fetal Health

There is no published experience in human fetuses. Quinapril likely crosses the human placenta like other ACEIs. As a group, adverse fetal effects are reported across gestation. In contrast to conclusions based on earlier data, adverse fetal effects occur even after 1st trimester exposure to ACEIs, for which the relative risk is 2.7. Exposure is associated with CV and CNS disorders. Later exposure is associated with cranial hypoplasia, anuria, reversible or irreversible renal failure, death, oligohydramnios, prematurity, IUGR, and PDA. The mechanism of renal dysfunction is likely related to fetal hypotension and prolonged decreased glomerular filtration. There is inadequate study to determine whether the response to quinapril is typical of this group. The one published rodent study is reassuring. If oligohydramnios is detected, quinapril should be discontinued unless lifesaving for the mother. Antenatal surveillance should be initiated (e.g., BPP) if the fetus is potentially viable. Oligohydramnios may not appear until after the fetus has irreversible injury. Neonates exposed in utero to ACEIs should be observed closely for hypotension, oliguria, and hyperkalemia. If oliguria occurs despite adequate BP and renal perfusion, exchange transfusion or peritoneal dialysis may be required.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Quinapril enters human breast milk with an M/P ratio of 0.12. No drug is detected more than 4h after maternal ingestion. It is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. There are no adequate reports or well-controlled studies of quinidine in pregnant women. All class IA agents should be administered with continuous cardiac monitoring in the hospital because of the risk of ventricular arrhythmia (torsades de pointes). Quinidine is a stereoisomer of quinine. It has a long record of safety during pregnancy, and is generally well tolerated. The clearance of quinidine is apparently unaffected by pregnancy. In women with severe P. falciparum malaria and hyperparasitemia, IV quinidine is often coupled with exchange transfusion, resulting in the clearing of the parasitemia and high survival rates. Therapeutic levels of quinidine inhibit pseudocholinesterase activity in pregnant women by 60-70%, necessitating caution if succinylcholine is to be used intraoperatively.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Quinidine crosses the human placenta, reaching an F:M ratio approaching unity over time. In vitro, it causes a dose-dependent relaxation of placental arteries and veins. Quinidine has been used successfully to correct fetal SVT and reverse hydrops. Elimination of maternal parasitemia does not necessarily mean elimination from the placenta. Rodent teratogenicity studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Quinidine is excreted into human milk with an M:P ratio near unity. It is estimated that the unsupplemented neonate would ingest 1.2mg/kg/d, or 1% of the total maternal daily dose. This is below the therapeutic dose prescribed to infants. Neonatal kinetics have not been studied.

Pregnancy

. Malaria is a major cause of maternal/perinatal morbidity and death in regions of the world. Treatment dramatically reduces those risks. Quinine is used extensively in developing countries for the treatment of malaria during pregnancy. Its metabolism and clearance are unaltered by pregnancy. It is one of a limited number of drugs used where multidrug-resistant P. falciparum is endemic. However, quinine has a higher treatment failure rate than chloroquine. Quinine toxicity is associated with abortion.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Quinine crosses the placenta, achieving an F:M ratio of 0.32 ? 0.14. The risks of

Pregnancy

loss, IUGR, or malformation are unchanged after 1st trimester exposure for malaria treatment. Congenital malformations reported in the human were associated with large doses (up to 30g) taken to trigger abortion. In about half of these reports, the abnormality was deafness related to auditory nerve hypoplasia. Other abnormalities reported included limb anomalies, visceral defects, and visual changes. Teratogenic effects are observed in rabbits and guinea pigs but not mice, rats, dogs, and monkeys. Congenital malaria is rare, but elimination of the maternal parasitemia does not guarantee elimination from the placenta. Quinine is used for the treatment of neonatal malaria. Considering the kinetics of placental transport, fetal toxicity seems a low probability at recommended doses.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Quinine enters human breast milk, achieving an M:P ratio of 0.31 (range 0.11-0.53). The total daily dose ingested by the unsupplemented neonate is between 1 and 3mg/d. There are no reports of toxicity in breastfed newborns.

Pregnancy

. GERD and/or heartburn occur in 45-85% of women during pregnancy. The effect of estrogen and progesterone on lower esophageal sphincter tone is a recognized factor. The treatment for GERD is the reduction of gastric acidity. There is no published experience with rabeprazole during pregnancy. Other proton pump inhibitors are generally considered effective treatment for GERD during pregnancy. There are no reported adverse effects. Proton pump inhibitors are first-line agents for the prevention of ??aspiration syndrome?? during general anesthesia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether rabeprazole crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether rabeprazole enters human breast milk. It is concentrated in rodent breast milk.

Pregnancy

. Over 50% of the rabies cases among Americans result from exposure to dogs outside the US. Prevention is key. Rabies is almost universally fatal once it occurs. Rabies immune globulin is prepared from the plasma of donors hyperimmunized with rabies vaccine. The product is standardized to an average potency of 150IU/ml. Rabies vaccine and rabies immune globulin should be given to all suspected of rabies exposure unless previously immunized with rabies vaccine and with confirmed adequate antirabies titers. It has been used successfully without complication during pregnancy. The reported adverse reaction rate is similar in pregnant and nonpregnant women.

Fetal Health

There are no adequate reports or well-controlled studies of rabies immune globulin in human fetuses. Antirabies IgG likely crosses the human placenta. Fetal infection with rabies is reported. It is not known whether transfer provides any level of protection to the perinate. Animal reproduction studies have not been performed.

Breastfeeding

There is no published experience in pregnancy. It is unknown whether rabies immune globulin enters human breast milk. However, other IgG antibodies are excreted into breast milk. 975

Pregnancy

. Over 50% of the rabies cases among Americans result from exposure to dogs outside the US. It is almost universally fatal once manifest. Rabies vaccine is an inactivated vaccine grown in chicken fibroblasts. Rabies vaccine and rabies immune globulin should be given to all suspected of rabies exposure unless previously immunized with rabies vaccine producing confirmed adequate antirabies titers. There are no data on the interchangeable use of different rabies vaccines in a single pre- or postexposure series. Thus, vaccine from a single manufacturer should be used for the complete series if possible. The vaccine has been used successfully during pregnancy, and pregnant women respond immunologically at least as well as nonpregnant women. 976 The reported adverse reaction rate is similar in pregnant and nonpregnant women.

Fetal Health

There are no adequate reports or well-controlled studies of rabies vaccine in human fetuses. Fetal rabies is reported. It is likely the IgG antibody produced in response to the vaccine crosses the placenta. It is not known whether transfer provides any level of perinatal protection. In one trial, intrauterine growth and

Pregnancy

outcome were normal in women vaccinated for postexposure prophylaxis. There were no adverse vaccine effects reported in over 250 pregnancies.

Breastfeeding

There is no published experience in nursing women. It is unknown whether rabies vaccine enters human breast milk. It is likely the antibodies produced in response to the vaccine are excreted into the milk. It is generally accepted that the woman can resume Breastfeeding once the vaccination series has begun.

Pregnancy

. The decline in estrogen after oophorectomy and menopause enhances bone resorption and accelerates bone loss. Osteoporosis is underdiagnosed and undertreated. SERMs are a new family of drugs for the management of estrogen-related pathology. Raloxifene decreases resorption of bone and reduces biochemical markers of bone turnover to the premenopausal range. Raloxifene does not stimulate the endometrium and may reduce the risk of ovarian cancer. It does not appear to affect the patient?s interest in sex, desire for or frequency of sexual activity, or the frequency or intensity of orgasm. Nor does raloxifene interfere with estrogen and non-hormonal vaginal cream moisturizers in postmenopausal vaginal atrophy. Long-term effects are under study. There is no published experience during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is not known whether raloxifene crosses the human placenta. Studies in rodents reveal an increase in several types of defects, including heart, brain, and skeleton. Different from estrogen, raloxifene does not alter the organization of the neuronal system related to sexual receptivity in rodents.

Breastfeeding

There is no published experience in nursing women. It is unknown whether raloxifene enters human breast milk.

Pregnancy

. Some ACEIs decrease proteinuria and preserve renal function in patients with hypertension and diabetes mellitus to a greater extent than other antihypertensive agents. More recently, they were shown to decrease the progression of nephropathy in normotensive patients with type 2 diabetes mellitus. There are no adequate reports or well-controlled studies of ramipril in pregnant women. In general, ACEIs are avoided during

Pregnancy

because of fetal risks. The lowest effective dose should be used if ramipril is required for BP control during pregnancy.

Fetal Health

There is no published experience in human fetuses. Ramipril likely crosses the human placenta as similar agents do. Transfer was described as low in one rodent study. In contrast to conclusions based on earlier data, adverse fetal effects occur even after 1st trimester exposure to ACEIs, for which the relative risk is 2.7. Exposure is associated with CV and CNS disorders. No such increase is seen with other classes of antihypertensive agents. Later exposure is associated with cranial hypoplasia, anuria, reversible or irreversible renal failure, death, oligohydramnios, prematurity, IUGR, and PDA. The mechanism of renal 979 dysfunction is likely related to fetal hypotension associated with prolonged decreased glomerular filtration. There is inadequate study to decide whether ramipril is typical of ACEIs. However, the one published rodent study is reassuring. If oligohydramnios is detected, ramipril should be discontinued unless lifesaving for the mother. Antenatal surveillance should be initiated (e.g., BPP) if the fetus is potentially viable. Oligohydramnios may not appear until after the fetus has irreversible injury. Neonates exposed in utero to ACEIs should be observed closely for hypotension, oliguria, and hyperkalemia. If oliguria occurs despite adequate pressure and renal perfusion, exchange transfusion or peritoneal dialysis may be required.

Breastfeeding

There is no published experience in nursing women. It is unknown whether ramipril enters human breast milk. It is described as low in rodents.

Pregnancy

. Pregnant women with symptomatic GERD should be managed aggressively with lifestyle and dietary modification. Antacids are first-line therapy. Should they fail, ranitidine or cimetidine are second-line options effective during pregnancy. Ranitidine has also been used successfully during

Pregnancy

for the treatment of Zollinger-Ellison syndrome. It is used in many labor wards every 6h to reduce the risk of acid aspiration.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Ranitidine crosses the human placenta, achieving in the isolated perfused cotyledon about 40% of the level of antipyrene. Epidemiologic study reveals no increased prevalence of adverse fetal outcomes following 1st trimester exposure. Rodent studies are reassuring, noting no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Ranitidine reduces fetal gastric pH when administered to pregnant rabbits, thus suggesting placental transfer.

Breastfeeding

There is no published experience in nursing women. While ranitidine is concentrated in human breast milk, no adverse effects are reported. Ranitidine is approved for use in pediatric practice.

Pregnancy

. Unlike other opioids, remifentanil undergoes rapid hydrolysis by nonspecific blood and tissue esterases. Even after a 4h infusion, the functional t/2 is only 4min. This characteristic suggests a potential for use in obstetrics. In a pilot study, remifentanil provided superior pain relief to laboring women when given by PCA compared to IM meperidine. However, remifentanil is difficult to titer in clinical practice, and produces high levels of sedation and excess rates of maternal oxygen desaturation. It is more often used as a supplement to neuraxial anesthesia during cesarean delivery.

Fetal Health

Remifentanil crosses the human placenta, achieving an F:M ratio approximating 0.5. Mean clearance approximates 93 ml/min/kg. Thus, while remifentanil crosses the placenta, it appears to be rapidly metabolized, redistributed, or both. Neonatal sedation is reported. Rodent studies are reassuring, revealing no evidence of 982 teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether remifentanil enters human breast milk. It is excreted into rodent breast milk. Considering the indication and t/2, one-time remifentanil use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. The published experience during

Pregnancy

with repaglinide is limited to isolated case reports. Its clearance is lower in women than in men. Insulin remains the standard agent for the treatment of hyperglycemia during pregnancy. However, a growing body of research indicates that some oral hypoglycemic agents such as glyburide may be equally effective and safe, while more convenient.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether repaglinide crosses the 983 human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity. However, an increased risk of IUGR may be secondary to chronic maternal hypoglycemia.

Breastfeeding

There is no published experience in nursing women. It is unknown whether repaglinide enters human breast milk. It does enter rat milk and is associated with skeletal deformities in the feeding pups.

Pregnancy

. Reserpine is a pure crystalline alkaloid of rauwolfia. It is a second-line agent for the treatment of hypertension. Reserpine is also used for the treatment of cerebral vasospasm, migraines, Raynaud?s syndrome, refractory depression, tardive dyskinesia, and thyrotoxic crisis. There is only limited study during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Reserpine crosses the human placenta. It can increase neonatal respiratory tract secretions, and cause nasal congestion, cyanosis, and anorexia. While it is unclear whether reserpine is a human teratogen, rodent studies reveal evidence of teratogenicity and embryotoxicity. It is also tumorigenic.

Breastfeeding

Reserpine is excreted in human breast milk. Increased respiratory tract secretions, nasal congestion, cyanosis, and anorexia can occur in breastfed infants.

Pregnancy

. Reteplase is recombinant plasminogen activator. There are no adequate reports or well-controlled studies of reteplase in pregnant women. The published experience is limited to 2 case reports associated with life-threatening thrombosis. There were no reported adverse effects. There is a real risk of uterine hemorrhage if administered in the puerperium.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether reteplase crosses the human placenta. Rodent studies showed no evidence of teratogenicity, but there was an increased risk of genital hemorrhage and abortion.

Breastfeeding

There is no published experience in nursing women. It is unknown whether reteplase enters human breast milk. However, considering the indication and dosing, one-time reteplase use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Rh alloimmunization remains a perinatal health problem even in countries with a developed program of prophylaxis. Patient or medical error is the most common cause of failed prophylaxis. Anti-D human immunoglobulin has been in clinical use for more than 30y. Its assessment is based more on experience than on well-designed comparative trials, but is estimated to have reduced perinatal mortality by about 10,000 cases/y in the US alone. A meta-analysis of 6 trials involving more than 10,000 women demonstrated efficacy of prophylaxis after delivery of a Rho(D)-positive infant to a Rho(D)-negative woman, reducing sensitization from 10% to 1.5%. The addition of antenatal prophylaxis reduces the rate of sensitization further, down to <0.5%. However, the optimal dosing regimen and route of administration remain unclear. Some data favor the use of Rho(D) immune globulin after abortion, as it appears to reduce immunization rates from about 3-4% to 0.4%. Rho(D) immune globulin is also likely effective antenatally in circumstances or procedures carrying a risk of maternal exposure to fetal RBCs, although this has not been proved in comparative trials. 987 Criteria for an Rh-incompatible

Pregnancy

requiring treatment includes: mother Rho(D)-negative, not previously sensitized to the Rho(D) factor; neonate Rho(D)-positive and direct antiglobulin negative. It is generally recommended that Rho(D) immune globulin should be administered to all nonsensitized Rh?women after spontaneous or induced abortion, ruptured tubal pregnancy, chorionic villus sampling, amniocentesis, abdominal trauma, or any occurrence of transplacental hemorrhage unless the fetus is known to be Rho(D)-negative. However, there is minimal evidence that administering Rh immune globulin for 1st trimester vaginal bleeding prevents maternal sensitization or development of hemolytic disease of the newborn. The practice is based on expert opinion and extrapolation from experience with fetomaternal hemorrhage in late pregnancy. Its use for 1st trimester bleeding is not evidence-based. If Rho(D) immune globulin is given antenatally, it is essential the mother receive another dose after delivery of a Rho(D)-positive infant. If the father is known and Rho(D)-negative, Rho(D) immune globulin is unnecessary. Rho(D) immune globulin should be given within 72h of delivery or abortion (spontaneous or iatrogenic). Passively acquired anti- Rho(D) may be detected after delivery following antenatal treatment; however, the woman should be treated again postpartum if the neonate is Rho(D)-positive. One 300mcg vial or syringe is sufficient to prevent maternal sensitization if the transferred fetal PRBC volume is <15ml (30ml whole blood). More than one vial or syringe of Rho(D) immune globulin must be given when the fetomaternal hemorrhage >15ml PRBCs or 30ml whole blood. The number of vials required is calculated by taking the volume of PRBCs determined by an approved laboratory assay, divided by 2 to get the volume of packed fetal RBCs in the maternal blood, and dividing that number by 15 to get the number of syringes or vials. More recently, it has been suggested that Rho(D) immune globulin might be helpful in women with ITP unresponsive to corticosteroids and nonspecific types of immune globulin.

Fetal Health

There is no evidence of fetal harm after extensive clinical experience. Babies born of women given Rho(D) immune globulin antepartum may have a weakly positive antiglobulin test at birth. There is no credible evidence that the risk of autism is increased by antenatal exposure.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Rho(D) immune globulin is excreted into human breast milk, but the amount of intact antibody detectable in the neonate is too low to cause clinically relevant hemolysis.

Pregnancy

. Hepatitis C is a growing problem worldwide. Perhaps1=3 of patients with HIV also have hepatitis C. Liver disease due to chronic HCV infection is now the 2nd leading cause of death in some HIV-infected populations. It is the most common cause of chronic liver disease and liver transplantation. The application of blood product screening has virtually eliminated transfusion-related viral transmission. As a result, maternal-fetal transmission is now one of the most important modes of transmission. HCV transmission is 2- to 4-fold higher in women co-infected with HIV. Cesarean delivery has not been shown to decrease perinatal transmission. The published experience with ribavirin during

Pregnancy

is limited to case reports. No adverse effects are reported. Considering the risk of viral transmission to the perinate is increased by co-infection, it seems likely future trials will address treatment of hepatitis C in HIV-infected pregnant women. The CDC does not recommend ribavirin for postexposure prophylaxis. Patients with chronic hepatitis whose therapy can be delayed should not be treated until controlled studies are available. However, women exposed to ribavirin inadvertently during

Pregnancy

may be encouraged to continue pregnancy. In patients with acute hepatitis C during pregnancy, the use of ribavirin therapy should be considered with close monitoring. The Ribavirin

Pregnancy

Registry was initiated in January 2004. 989

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether ribavirin crosses the human placenta. There are only limited case reports of its use during pregnancy. Rodent studies reveal an increased prevalence of limb, eye, and brain defects. The incidence and severity is proportional to drug dose. Teratogenicity was not seen at doses approximating the recommended human dose. Ribavirin is often used in the pediatric population for the treatment of RSV. The prevalence of hepatitis C in children is between 0.05% and 0.4%. The major mode of acquisition has shifted from parenteral to maternal-infant transmission. While the actual rate of maternal-infant transmission is low, HIV increases the rate of transmission.

Breastfeeding

There is no published experience in nursing women. It is unknown whether ribavirin enters human breast milk. Ribavirin is toxic to lactating rats and their offspring.

Pregnancy

. Riboflavin is an important nutrient contained in virtually all multivitamin supplements. Contrary to conventional wisdom, the maternal concentration of riboflavin does not decline during normal, unsupplemented pregnancy. However, maternal supplementation does generate supraphysiologic levels. Epidemiologic studies suggest multivitamin supplementation during the

Pregnancy

of HIV-infected women improves maternal weight gain.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Riboflavin is actively transported across the human placenta with a transfer index (clearance riboflavin:clearance L-glucose) in the isolated cotelydon of 3.4 ? 0.95. Observational studies note a positive relationship between maternal riboflavin levels and fetal size. This finding also applies to women who abuse tobacco. There is no substantative evidence riboflavin is a teratogen, though epidemiological study suggests low intake may be associated with congenital heart disease. In some animal models, riboflavin supplementation reduces the incidence of NTDs.

Breastfeeding

Riboflavin is excreted into human breast milk, and the concentration is proportional to the maternal concentration. Women who do not drink milk are more likely to have low concentrations of riboflavin in their breast milk.

Pregnancy

. Rifabutin is an alternative to rifampin for the treatment of Mycobacterium TB in HIV-infected women taking certain antiretroviral agents concomitantly. It is also recommended by the U.S. Public Health Service/Infectious Diseases Society of America Prevention of Opportunistic Infections in Persons Infected with HIV Working Group as an alternative agent to rifampin for chemoprophylaxis of tuberculosis. There is no experience with rifabutin during pregnancy. In healthy nonpregnant women, rifabutin and rifampin significantly increase the clearance of ethinyl estradiol, suggesting women who use low-dose oral contraceptives should either switch to a higher dose or use a backup contraceptive method while taking rifabutin.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether rifabutin crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether rifabutin enters human breast milk. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. Untreated TB poses a significant threat to the mother, fetus, and family. A 3-drug regimen of rifampin, isoniazid, and pyrazinamide is recommended for the initial 2mo treatment phase. All pregnant women taking isoniazid should also take pyridoxine 993 to reduce the chance of a ?chemical? hepatitis. The CDC recommends that either streptomycin or ethambutol be added during the initial treatment unless the likelihood of isoniazid resistance is low. However, streptomycin is contraindicated in pregnancy. Ciprofloxacin has the best safety profile of second- line drugs for the treatment of drug-resistant TB. After the initial phase, treatment is continued with rifampin and isoniazid for 4mo, or longer if the sputum or culture is positive, resistant organisms are present, or patient is HIV positive. There are no adequate reports or well-controlled studies of rifampin in pregnant women. A long clinical experience suggests

Pregnancy

does not increase the risk of an adverse effect. Rifampin may cause hemorrhage in the mother and neonate when administered during the 3rd trimester. Treatment with vitamin K may be indicated. Rifampin impairs the effectiveness of OCPs. Women using a low- dose OCP should consider a higher dose preparation or a backup method of contraception.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Rifampin crosses the human placenta, but the kinetics have not been detailed. There is no substantative evidence of teratogenicity in humans. Rifampin does cross the rodent placenta, and is teratogenic at oral doses 15-25the MRHD, affecting bone, spine, and palate, depending upon the species. Congenital TB does occur on occasion, especially in association with miliary TB. Rifampin is used to treat children in the first few months of life.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only trace amounts of rifampin are excreted into human breast milk.

Pregnancy

. Rifapentine is similar to rifampin, but has a more convenient dosing protocol. It must be taken in tandem with at least one other antituberculosis drug to which the isolate is susceptible. There are no adequate reports or well-controlled studies of rifapentine in pregnant women. The published experience is limited to isolated case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Rifapentine is teratogenic in rodents when given 995 at doses similar to human, affecting bone, heart, spine, and palate (species-dependent). There is also evidence of embryotoxicity.

Breastfeeding

There is no published experience in nursing women. It is unknown whether rifapentine enters human breast milk.

Pregnancy

. ALS is the most common progressive motor neuron disease, but is rare in the obstetric population. There are no published reports of riluzole use during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether riluzole crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Maternal and embryo toxicity were seen.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether riluzole enters human breast milk.

Pregnancy

. Pregnant women suffered a higher mortality rate during the influenza pandemics of the last century and should be vaccinated prior to each influenza season. Prophylaxis is not a substitute for vaccination, although it is an important adjunct. Rimantadine is 70-90% effective in preventing influenza A. When used for prophylaxis, antiviral agents can prevent illness while permitting subclinical infection and the genesis of protective antibodies. Rimantadine reduces the duration of the illness if administered within 2d of symptom onset should an unprotected woman contract influenza A. To reduce the emergence of antiviral drug?resistant viruses, rimantadine therapy is discontinued as soon as clinically warranted, typically after 3-5d, or within 24-48h from resolution of signs and symptoms. There is no published experience with rimantadine in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether rimantadine crosses the human placenta. It does cross the rodent placenta and is initially concentrated in the fetal liver. The elimination t/2 is less than 3h. Rodent studies are generally reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryo and maternal toxicity occur at the highest doses. There is also an increase in pup death during the first 2-4d postpartum, and decreased fertility of the F1generation. Rimantadine has not been tested in children under 1y.

Breastfeeding

There is no published experience in nursing women. It is unknown whether rimantadine enters human breast milk. Rimantadine is concentrated in rat milk in a dose-dependent fashion, achieving twice plasma levels 2-3h after dosing. Until further study, Breastfeeding women who choose to take rimantadine should probably stop feeding and pump until 48h after discontinuing the drug.

Pregnancy

. There is no published experience with risedronate during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether risedronate crosses the human placenta. In one study, placental transport was not confirmed in the mouse. Rodent studies are generally reassuring, revealing no clear evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Pregnancy

wastage was increased with maternal toxicity.

Breastfeeding

There is no published experience in nursing women. It is unknown whether risedronate enters human breast milk. Small amounts are excreted into rodent milk.

Pregnancy

. There are no adequate reports or well-controlled studies of risperidone in pregnant women. The published experience is limited to several case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether risperidone crosses the human placenta. The

Pregnancy

outcomes of women who contacted a teratogen information service and the manufacturer?s data after exposure to risperidone appeared normal. It does cross the rodent placenta. Rodent studies are generally reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. The observed increased neonatal mortality may relate to either the drug or maternal toxicity.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Risperidone enters human breast milk. In one woman taking 6mg PO qd, the peak milk levels of risperidone and its active metabolite were 12mcg/L and 40mcg/L, respectively. Thus, the estimated infant dose is 7.8mcg/kg/d, or 4.3% of the weight-adjusted maternal dose. There are case reports of its use in Breastfeeding women without apparent adverse effect.

Pregnancy

. Preterm delivery is the leading cause of perinatal morbidity and death. There is no tocolytic agent known to change

Pregnancy

outcome short of allowing corticosteroid administration. Ritodrine decreases the intensity and frequency of uterine contractions, but does not alter in a clinically relevant fashion the 1001 gestational age at delivery compared to placebo. Though the first drug approved as a tocolytic in the US, it was withdrawn from the market by its manufacturer. It is inferior to either nifedipine or atosiban in terms of both delivery delay and maternal morbidity. Ritodrine produces an immediate dose-related elevation of HR with maximum mean increase of 19-40bpm. The pulse pressure widens, the average systolic pressure increases 4.0mmHg, and the average diastolic pressure decreases 12.3mmHg. IV infusion transiently elevates glucose, insulin, and free fatty acids, while serum potassium declines. Maternal pulse rate and BP and FHR should be closely monitored. The effectiveness of parenteral ritodrine for tocolysis is limited to short-range prolongation of gestation. The effectiveness of maintenance tocolytic therapy with oral ritodrine is not proved. Maternal signs and symptoms of pulmonary edema should be sought constantly. A persistent tachycardia (>140bpm) may be a sign of impending pulmonary edema. Occult cardiac disease may be unmasked by ritodrine. If the patient complains of chest pain or tightness of chest, the drug should be temporarily discontinued. A baseline ECG is not cost-effective. Ritodrine has also been used to facilitate external version of a breech fetus.

Fetal Health

Ritodrine crosses the human placenta. There is no evidence of teratogenicity in humans. Rodent studies are reassuring. It has been suggested that ritodrine and other b-mimetics might promote fetal growth. This hypothesis cannot be confirmed. Ritodrine increases the FHR and left cardiac output, and has been used to treat fetal complete heart block.

Breastfeeding

There is no published experience with ritodrine in pregnancy. However, considering the indication and clearance, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. There are few well-controlled studies of ritonavir in pregnant women. Published cohort studies and case reports do not suggest an increased risk of an adverse outcome during pregnancy. Many commonly used drugs alter the clearance of ritonavir. The patient should be questioned closely about concurrent drug use before prescribing.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Placental transport of ritonavir is very low; most umbilical cord samples studied are below the level of detection. Limited transfer for most protease inhibitors reflects both their 1003 high degree of plasma protein binding and their backward transport by P-glycoprotein in the placenta. Rodent studies are generally reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Combination therapy may enhance toxicity. Maternal toxicity from high doses leads to embryo toxicity.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether ritonavir enters human breast milk. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. Rivastigmine is believed to enhance cholinergic function by increasing ACh concentration in the intact cholinergic nerves, keeping them functionally intact. There is no evidence that rivastigmine alters the course of the underlying disease. Clearance is altered by renal disease, though it is unclear whether the dose needs to be adjusted in response. There is no published experience with rivastigmine during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether rivastigmine crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than that used clinically. In pregnant rabbits receiving multiple PO doses, the fetus:placental tissue ratio of radioactivity averaged 0.5. 1006

Breastfeeding

There is no published experience in nursing women. It is unknown whether rivastigmine enters human breast milk. Only metabolites of the active drug were found in rabbit breast milk.

Pregnancy

. There is no published experience with rizatriptan during pregnancy. Clearance is slower in nonpregnant women compared to men.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether rizatriptan crosses the human placenta. A review of the outcomes of 25 prospective reports in the

Pregnancy

Registry and other sources does not suggest rizatriptan predisposes to either spontaneous abortions or congenital anomalies. Rodent studies are generally reassuring, revealing no evidence of teratogenicity. However, embryo toxicity and IUGR were noted unrelated to maternal toxicity. 1007

Breastfeeding

There is no published experience in nursing women. It is unknown whether rizatriptan enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of rocuronium in pregnant women, though it has been used for cesarean delivery as part of rapid-sequence general anesthesia in patients who have a contraindication to succinylcholine (e.g., suspected malignant hyperthermia, upper-motor neuron lesion). However, the manufacturer notes that tracheal intubation can be problematic 60sec after administration, and does not recommend 1008 its use (i.e., replacing succinylcholine) for rapid-sequence induction of general anesthesia for cesarean delivery. Rocuronium neuromuscular blockade may be prolonged by magnesium sulfate infusion or in the postpartum period if dosing is based on total rather than lean body weight.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Rocuronium crosses the human placenta. In women undergoing rapid-sequence induction of general anesthesia, the F:M ratio approximates 0.18 at delivery. No clinical sequelae are noted. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically, assuming the mother was properly oxygenated.

Breastfeeding

There is no published experience in nursing women. However, considering the indication and dosing, limited use of rocuronium is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Rofecoxib was withdrawn from the market in 2004. It is a COX- 2 inhibitor that has analgesic, anti-inflammatory, and antipyretic properties. Because of its lack of platelet effects, rofecoxib is not a substitute for aspirin for CV prophylaxis. It is no more effective than diclofenac and ibuprofen for the relief of mild to moderate pain when used at maximal doses. Further, it only modestly reduces the risk of GI reactions (1.3% vs. 1.8% after 1y of treatment). There are no adequate reports or well-controlled studies of rofecoxib in pregnant women. Though rofecoxib inhibits spontaneous contractions of isolated rat myometrium at lower concentrations than indomethacin, it has no effect on either the onset or duration of labor in rodents. 1010

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Rofecoxib crosses the human placenta. Fetal levels are dependent on maternal, as NSAID agents are not metabolized by the fetal kidney. Similar to other NSAIDs, rofecoxib is associated with oligohydramnios and constriction of the ductus arteriosus. The latter reverses with cessation, and the long-term impact of in utero ductal constriction on the otherwise healthy fetus is currently unknown. Rodent studies are generally reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity was noted at higher doses.

Breastfeeding

Rofecoxib (25mg) was given to 6 women at weaning. Blood and milk were sampled up to 72h postdose. The median (range) M:P ratio and infant ??dose?? were 0.25 (0.16-0.32) and 2.1% (1.8-3.2%), respectively. Thus, the use of rofecoxib during Breastfeeding is unlikely to pose harm based on the low transfer into human milk.

Pregnancy

. There is no published experience with ropinirole during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether ropinirole crosses the human placenta. Rodent teratogenicity studies reveal IUGR and digit abnormalities at doses that are multiples of the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether ropinirole enters human breast milk. Ropinirole inhibits prolactin secretion in humans and could interfere with establishment of the milk reflex.

Pregnancy

. Rosiglitazone may be used alone or in combination with metformin or a sulfonylurea. The short-term use of rosiglitazone and clomiphene is more efficacious than metformin and clomiphene for ovulation induction in women with clomiphene- resistant PCOS. Improved glucose control may also lead to ovulation in premenopausal, anovulatory women and increase the risk of an unplanned pregnancy. Paradoxically, it may interfere with ovulation in spontaneously cycling women. Concern that rosiglitazone may increase the risk of adverse cardiac events remains controversial. The published experience with rosiglitazone during

Pregnancy

is limited to case reports and small series.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Rosiglitazone crosses the human placenta. In a study of women undergoing elective abortion, drug transfer increased after 10w, achieving roughly a 2:1 M:F concentration gradient. Minimal amounts of rosiglitazone in AF suggest fetal metabolism. In another study employing the dual perfused isolated placental cotelydon, the clearance indices for low and high concentrations of rosiglitazone were 0.14 ? 0.04 and 0.20 ? 0.08, suggesting the drug crosses the placenta at a relatively low rate. Fetal accumulation occurred in only 1/5 placentas at 16.4ng/ml (5%) for an 8mg dose and in 2/5 placentas ranging from 0 to 74ng/ml (5% to 8%) at higher concentrations. Rodent studies are generally reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. High doses were associated with fetal losses and IUGR, possibly reflecting sustained hypoglycemia. 1013

Breastfeeding

There is no published experience in nursing women. It is unknown whether rosiglitazone enters human breast milk. It is excreted into rat milk.

Pregnancy

. The rubella virus vaccine produces a modified, noncommunicable rubella infection in susceptible persons. Vaccine-induced immunity persists for at least 10y without significant decline. Vaccinating susceptible women confers individual protection against rubella during a subsequent pregnancy, thus preventing congenital rubella. Yet, only about half the world?s countries vaccinate for rubella. Outbreaks continue to occur in countries with national immunization programs, typically involving women born in other countries. 1014 Perhaps the most convenient time to vaccinate is immediately postpartum while the patient is still hospitalized. In that instance, conception should be delayed 1mo. Unfortunately, the opportunity is often missed because of physician/hospital oversight. Rubella susceptibility should be confirmed serologically before vaccinating.

Fetal Health

Rubella vaccine virus has been found in the products of conception in women undergoing termination and in the offspring of vaccinated women. Similar to natural viral infections, newborns may shed virus for an extended time. The manufacturer reports that in over 700 women inadvertently vaccinated within 3mo before or after conception, no newborn had stigmas of congenital rubella syndrome.

Pregnancy

termination is not recommended solely because of inadvertent vaccination.

Breastfeeding

Rubella vaccine virus is excreted into human breast milk, and neonatal infection is reported. However, the risk is generally considered small and immunization not a reason to avoid breastfeeding.

Pregnancy

. Asthma is estimated to affect up to 4% of pregnancies. For pregnant women with persistent asthma, inhaled cromolyn is generally considered the first-line therapy, followed by inhaled budesonide if symptoms worsen. Salmeterol is a long-acting b-adrenergic agonist. It also is a potent inhibitor of mast cell release of histamine, leukotrienes, and prostaglandin D2. Systemic levels of salmeterol are low or undetectable after inhalation. It has also been used for the treatment of altitude sickness. There are no published trials of its use during pregnancy, and recommendations are based on ??expert?? opinion. It is typically used as a secondary agent.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether salmeterol crosses the human placenta. Transfer across the rat placenta is low. Considering the low systemic levels achieved and the poor placental transport, it is unlikely the fetus is exposed to a clinically relevant concentration. When given orally at doses 50-100greater than those inhaled, salmeterol is associated with cleft palate and abnormal ossification. These studies do not seem relevant to clinical practice.

Breastfeeding

There is no published experience with salmeterol in Breastfeeding women. However, considering the dose and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts. The transfer into rodent milk is limited.

Pregnancy

. Salsalate is a dimer of salicylic acid and absorbed in the intestine. Unlike aspirin, salsalate does not inhibit platelet aggregation, and there is no increase in GI bleeding over placebo. There is no published experience during pregnancy.

Fetal Health

There is no published experience in human fetuses. It is unknown whether salsalate crosses the human placenta. Salsalate and salicylic acid are teratogenic and embryocidal in rats when given in doses 4-5the usual human dose; teratogenicity is not seen when given at twice the usual human dose.

Breastfeeding

There is no published experience in nursing women. It is unknown whether salsalate enters human breast milk. Salicylic acid, the primary metabolite, reaches an M:P ratio approximating unity. 1017

Pregnancy

. Saquinavir is well-tolerated during

Pregnancy

and is part of several treatment regimens. Its clearance is increased by pregnancy, and the usually recommended dose may be inadequate. Ritonavir significantly increases saquinavir concentration, and the combination during

Pregnancy

may have some advantage.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Saquinavir, like many protease inhibitors, does not significantly cross the human placenta probably because of reverse placental P-glycoprotein transport whose expression 1018 it enhances. Unbound concentrations of saquinavir are likely to be substantially lower in umbilical cord than maternal plasma. It is unlikely to pose a significant risk to the fetus. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR.

Breastfeeding

There is no published experience in nursing women. It is unknown whether saquinavir enters human breast milk. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. Sargramostim is a recombinant human granulocyte-macrophage colony-stimulating factor. There is no published experience with sargramostim during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether sargramostim crosses the human placenta. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There is no reported experience in nursing women. It is unknown whether sargramostim enters human breast milk.

Pregnancy

. Scopolamine differs only quantitatively in antimuscarinic actions from atropine. It is ineffective for the prevention of postoperative N/V. At one time popular for ??twilight sleep?? during labor, scopolamine has appropriately fallen out of favor. A recent study suggests it is effective in reducing the duration of the first stage of labor, and was not associated with any obvious adverse outcomes. It may reduce the post?cesarean section N/V associated with epidural morphine, but with an increase in drowsiness and dry mouth. Scopolamine is rapidly cleared, but there is no significant relationship between HR changes, sedative effects, and antisialagogue effects and serum concentration.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Scopolamine rapidly crosses the human placenta and may cause tachycardia and decreased beat-to-beat and long- term variability. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Scopolamine enters human breast milk, but the kinetics remain to be elucidated. The long clinical experience is reassuring.

Pregnancy

. Barbiturates are dangerous drugs, with a narrow therapeutic index between the level required for sedation and that causing coma and death. Secobarbital is used by patients to self-treat the unpleasant effects of illicit stimulants, to reduce anxiety, and to get ??high.?? It is physiologically addicting if taken in high doses for 1mo or more, and the abstinence syndrome can be life- threatening. There are no adequate reports or well-controlled studies of secobarbital in pregnant women. As a short-acting agent, secobarbital was used for decades as a short-term sleeping aid for pregnant women. Unfortunately, the sleep produced is not restful, characterized by a low percentage of REM stage. Hypnotic doses of barbiturates do not impair uterine activity significantly during labor. Anesthetic doses of barbiturates decrease the force and frequency of uterine contractions. 1023

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is likely secobarbital rapidly crosses the human placenta. There is no substantative evidence secobarbital is a human teratogen. Administration during labor may cause respiratory depression in the newborn. Premature infants are particularly susceptible to the depressant effects of barbiturates. Withdrawal symptoms occur in infants of women who receive secobarbital throughout the 3rd trimester.

Breastfeeding

There is no published experience in nursing women. Small amounts of secobarbital are excreted into human breast milk, but its occasional use is generally considered compatible with breastfeeding.

Pregnancy

. Selegiline is a derivative of phenethylamine. It has also been used for the treatment of Alzheimer?s dementia and narcolepsy. There are no adequate reports or well-controlled studies of selegiline in pregnant women. The literature consists of case reports involving 30-40 women in total with Parkinson?s disease.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether selegiline crosses the human placenta. Monoamine neurotransmitters are important for the development of the immature brain. Their endogenous levels are highly regulated by MAO, and any change in enzyme activity could have a profound effect on brain development. Some recommend discontinuing MAOIs before conception. Unfortunately, there is little scientific information on which to base such decisions. Rodent studies are generally reassuring, revealing no evidence of teratogenicity at doses higher than those used clinically. There was evidence of embryotoxicity at high doses.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether selegiline enters human breast milk.

Pregnancy

. There is no published experience with selenium sulfide during pregnancy. Systemic absorption is scant whether measured after shampooing or lotion application.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether selenium sulfide crosses the human placenta. Elemental selenium does cross passively. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level.

Breastfeeding

There is no published experience in nursing women. It is unknown whether selenium sulfide enters human breast milk. However, the concentration of elemental selenium in milk is the same as maternal plasma. Considering the indication and dosing, selenium sulfide use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Despite a long clinical experience, there are no adequate reports or well-controlled studies of senna in pregnant women. Senna is absorbed across the GI tract only to a limited degree. Some believe senna is the purgative of choice during

Pregnancy

and lactation. It effectively relieves postpartum constipation. It does not affect the myometrial activity of the pregnant ewe.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether senna crosses the human placenta. 1027

Breastfeeding

Less than 1% of the maternal dose of senna enters human breast milk. This amount is inadequate for a clinical effect.

Pregnancy

. Depression is common during and after pregnancy, but typically goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. There are no adequate reports or well-controlled studies of sertraline in pregnant women, though there is growing experience with its use for the treatment of postpartum depression. However, sertraline is not recommended for prophylactic use. In general, women taking SSRIs during

Pregnancy

for depression require an increased dose to maintain euthymia. Yet in the one longitudinal study clearance was unaltered during pregnancy. 1028

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Sertraline crosses the human placenta and enters the AF. Limited study suggests a low F:M ratio approximating 0.30-0.67, lower than citalopram, fluoxetine, and paroxetine. Maternal doses predict the umbilical cord concentration. Though there remains controversy, the most recent epidemiologic analyses reveal a significant association with omphalocele (OR, 5.7; 95% CI, 1.6-20.7; 3 exposed subjects) and septal defects (OR, 2.0; 95% CI, 1.2-4.0; 13 exposed subjects). An increased prevalence of IUGR cannot be excluded. Neonatal abstinence syndrome may occur in up to1=3 of exposed neonates. There is some concern that the impact of antenatal exposure continues for at least a few months. Newborns chronically exposed to SSRIs have reduced responses to pain. Rodent studies are generally reassuring, though a delay in ossification was noted in rabbits. Further, the fetal loss rate is increased by late

Pregnancy

exposure. The mechanism and significance are unclear. The exposure of mouse embryos in culture to sertraline at a high concentration (10mM) causes craniofacial malformations without evidence of general embryotoxicity, consistent with a direct action at 5-HT uptake sites.

Breastfeeding

Sertraline and desmethylsertraline are present in human breast milk. The concentrations are affected by the fraction of milk sampled, the time after maternal dose (max 7-10h), and daily dose. The mean maximum calculated nursing infant doses of sertraline (0.67mg/d) and desmethylsertraline (1.44mg/d) represent 0.54% of the maternal daily dose. Neonatal serum concentration is usually below the detection limit of most commercial laboratories. If breastfed, the infant should be monitored for possible adverse effects, the drug given at the lowest effective dose, and Breastfeeding avoided at times of peak drug levels.

Pregnancy

. There are no adequate reports or well-controlled studies of sevoflurane in pregnant women. It is popular for cesarean delivery when general anesthesia is elected, producing an intraoperative course and neonatal outcome similar to that of either isoflurane or a subarachnoid block. Like the other volatile anesthetics (halothane and isoflurane), sevoflurane reduces oxytocin-induced contraction of pregnant rat myometrium mediated, at least in part, by activation of Ca2+-activated K+channels. In vitro, it is a vasodilator of chorionic plate vessels. A limited number of case reports in the 1st trimester do not report adverse outcomes.

Fetal Health

Sevoflurane rapidly crosses the human placenta. It has been used for fetal anesthesia during the EXIT procedure. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR. Neonatal adaptive capacity may be reduced during the first 24h compared to desflurane.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether sevoflurane enters human breast milk. However, considering the indication and 1031 dosing, one-time sevoflurane use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Obesity is a major epidemic in the industrialized countries. Observational studies confirm a relationship between obesity and CV disease, type 2 diabetes mellitus, certain forms of cancer, gallstones, certain respiratory disorders, and an increase in overall mortality rate. These studies suggest that weight loss, if maintained, may produce health benefits for patients with chronic obesity. Sibutramine leads to dose-dependent weight loss. Maintenance therapy enhances the likelihood of maintaining the loss. The published experience during

Pregnancy

is limited to case reports and small series. Clearance is modestly decreased in women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether sibutramine crosses the human placenta. Case reports and small series are reassuring. Rodent studies are generally reassuring, with dysmorphology noted only at the highest doses concurrent with maternal toxicity and only in rabbits. Transport across the rodent placenta is limited.

Breastfeeding

There is no published experience in nursing women. It is unknown whether sibutramine enters human breast milk.

Pregnancy

. Sildenafil is suggested as a treatment for sexual arousal disorder in premenopausal women. It is effective in postmenopausal women for the treatment of female sexual arousal disorder. Though there are no adequate reports or well-controlled studies of sildenafil in pregnant women, it is a potentially attractive agent as it increases the t/2 of NO, and there are several reports of its use to treat pulmonary artery hypertension during pregnancy. Sildenafil has also been tested as an agent to increase uterine blood flow and endometrial development in women undergoing IVF.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether sildenafil crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. There is some interesting study using sildenafil as an agent to minimize the impact of acute perinatal asphyxia.

Breastfeeding

There is no published experience in pregnancy. It is unknown whether sildenafil enters human breast milk.

Pregnancy

. Silver nitrate has been used for decades to prevent neonatal gonorrheal conjunctivitis. Unfortunately, it does not prevent chlamydial conjunctivitis and has been largely replaced with erythromycin ointment.

Fetal Health

Not relevant

Breastfeeding

Not relevant

Pregnancy

. While burn injuries to pregnant women are not rare, the literature is indeed sparse. There are no adequate reports or well-controlled studies of silver sulfadiazine in pregnant women. Absorption of silver sulfadiazine varies depending upon the percentage of body surface area and the extent of the tissue damage.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether silver sulfadiazine crosses the human placenta. Considering the route and concentration, it is unlikely the maternal systemic concentration will reach a clinically relevant level. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether silver sulfadiazine enters human breast milk. Considering the route and concentration, it is unlikely the breastfed neonate will ingest a clinically relevant amount.

Pregnancy

. Simethicone significantly reduces vomiting, stomach discomfort, and abdominal pain post-cesarean section. Bowel function appears to return more rapidly.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. While it is unknown whether simethicone crosses the human placenta, it is unlikely the maternal systemic concentration reaches a clinically relevant level. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. While it is unknown whether simethicone enters human breast milk, it is unlikely the maternal systemic concentration reaches a clinically relevant level. It is generally considered compatible with breastfeeding.

Pregnancy

. Simvastatin is a synthetic statin that reduces the overall lipid level and the associated risk of adverse CV events. It may modestly increase the risk of cholelithiasis. Simvastatin does not affect gonadotropin function in premenopausal women. There are no adequate reports or well-controlled studies of simvastatin in pregnant women. Post-marketing studies do not suggest an increase in adverse outcomes. However, atherosclerosis is a chronic process. Discontinuation during

Pregnancy

should have little impact on the long-term therapeutic outcome of primary hypercholesterolemia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether simvastatin crosses the human placenta. Post-marketing studies are reassuring, as are rodent studies, which reveal no evidence of teratogenicity despite doses that were multiples of the MRHD. Inadvertent exposure would not be a medical indication for

Pregnancy

termination. However, cholesterol and other products of the cholesterol biosynthesis pathway are essential components for fetal development. In vitro, simvastatin sharply inhibited migration of extravillous trophoblast from villi into matrigel. Further, it inhibited half of the proliferative events in the villi and increased apoptosis of cytotrophoblast cells compared to control. Finally, simvastatin significantly decreased secretion of progesterone from the placental explants. Thus, exposed pregnancies may be at increased risk for IUGR. It is generally considered the potential fetal risk of simvastatin use outweighs the benefit to the mother.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether simvastatin enters human breast milk.

Pregnancy

. A growing number of obstetric patients have benefited from organ transplant.

Pregnancy

is considered reasonable if the patient is 2y post-transplantation, has good renal function without proteinuria, no uncontrolled arterial hypertension, and no evidence of ongoing rejection. Adverse outcomes are otherwise common and these pregnancies should be managed in a tertiary care center. The clearance of sirolimus is modestly increased in women. There are no adequate reports or well-controlled studies of sirolimus in pregnant women. The published experience is limited to case reports and moderate-sized series. It is generally avoided in favor of tacrolimus or azathioprine with or without steroids.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether sirolimus crosses the human placenta. Early

Pregnancy

exposure has not been associated with an increased risk of structural malformations. Sirolimus is embryotoxic in rodents. In vitro, it inhibits the growth of fetal myocardial cells.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether sirolimus enters human breast milk. Trace amounts are found in rat milk, and in vitro, sirolimus inhibited milk production.

Pregnancy

. There are no adequate reports or well-controlled studies of sodium bicarbonate in pregnant women. There is no reason to expect

Pregnancy

alters the risk of its use. It is most often used during

Pregnancy

in association with the treatment of DKA. There are also rare reports of its use for pica resulting in severe hypokalemic metabolic alkalosis and rhabdomyolysis.

Fetal Health

There are no adequate reports or well-controlled studies of sodium bicarbonate in human fetuses. Bicarbonate ions do equilibrate across the human placenta. There is no physiologic reason to expect a gradual correction of a metabolic acidosis would threaten the fetus. It is used during RBC transfusion of the profoundly anemic fetus to prevent severe acidemia and to resuscitate during fetal surgery. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether infused sodium bicarbonate enters human breast milk and increases milk concentration.

Pregnancy

. Sodium ferric gluconate is a stable macromolecular complex in sucrose injection. There is no adequate published experience with sodium ferric gluconate complex during pregnancy. Anaphylaxis has been reported during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether sodium ferric gluconate complex crosses the human placenta. Iron is transported across. There is no physiologic reason to expect an adverse effect if maternal iron content is in the normal range.

Breastfeeding

There is no published experience in nursing women. It is unknown whether sodium ferric gluconate complex enters human breast milk. However, iron is a normal component of breast milk, and other iron supplements increase the milk concentration.

Pregnancy

. There is no published experience with sodium polystyrene during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Sodium polystyrene is not absorbed systemically and should pose no direct risk to the fetus. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience with sodium polystyrene in nursing women. However, the low maternal systemic concentration precludes a direct effect.

Pregnancy

. There are no adequate reports or well-controlled studies of sotalol in pregnant women. The published literature is limited to case reports. Sotalol reduces BP in hypertensive women, but its reported use during

Pregnancy

is restricted to its properties as an antiarrhythmic agent.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Sotalol crosses the human placenta, reaching an F:M ratio approximating unity, and is found in AF. It has been used to treat fetal tachyarrhythmia where the mean F:M sotalol plasma concentration is 1.1 (range, 0.67-2.87; SD, 0.63), and the mean AF:fetal blood ratio is 3.2 (range, 1.28-5.8; SD, 1.4). The response rate exceeded 75% in the largest report. The effectiveness of sotalol, however, cannot be extrapolated from maternal blood levels. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. In rabbits, high doses are associated with embryonic death most likely secondary to embryonic arrhythmia.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Sotalol enters human breast milk. Mean M:P ratios of 2.4-5.4 are reported, with milk levels ranging from 5 to 20.2mg/L. There was no consistent difference in sotalol concentration between pre- and postfeed milk samples. Using an 1044 average milk intake of 0.15L/kg/d, it was calculated that an infant would have received a dose some 20-23% of the maternal dose. This dose was not associated with any bradycardia. However, because of the relatively large infant exposure to the drug, Breastfeeding should be undertaken only when the infant is closely monitored and

Pregnancy

. Spectinomycin is not effective for the treatment of syphilis, and may in fact mask or delay the symptoms of incubating syphilis. All patients with gonorrhea should be serologically tested for syphilis at diagnosis, and again 3mo later. There are no adequate reports or well-controlled studies of spectinomycin in pregnant women. Failure to achieve ??microbiologic cure?? is similar for common antibiotic regimens: amoxicillin plus probenecid compared with spectinomycin (OR 2.40, 95% CI 0.71-8.12), amoxicillin plus probenecid compared with ceftriaxone (OR 2.40, 95% CI 0.71-8.12), and ceftriaxone compared with cefixime (OR 1.22, 95% CI 0.16-9.04). Thus, the selection is based on sensitivities in the geographic locale, price, and the prevalence of syphilis. Sex partners should be tested and treated when possible.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether spectinomycin crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether spectinomycin enters human breast milk. Considering the likely dosage and that other aminoglycosides are generally considered safe for breastfeeding, the same should be true for spectinomycin.

Pregnancy

. Spironolactone increases sodium and water excretion while retaining potassium. There are no adequate reports or well- controlled studies of spironolactone in pregnant women. Diuretics should not be used to treat the physiologic edema of

Pregnancy

and do not prevent preeclampsia. There are superior agents for such off-label indications as hirsutism. It has been used for the treatment of maternal Bartter?s syndrome during

Pregnancy

with success.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether spironolactone crosses the human placenta. Spironolactone is an antiandrogen and can feminize male rats. However, there is at least one case report of an appropriately developed male newborn after high-dose treatment for maternal Bartter?s syndrome.

Breastfeeding

While spironolactone and its major active metabolite enter human breast milk, it is estimated that the Breastfeeding neonate would ingest <0.5% of the daily maternal dose.

Pregnancy

. Stavudine is a synthetic thymidine nucleoside analog. There are no adequate reports or well-controlled studies of stavudine in pregnant women. Mean maternal pharmacokinetics are unaffected by labor.

Pregnancy

increases the risk of potentially fatal lactic acidosis/hepatic steatosis when combined with didanosine and other antiretroviral agents.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Stavudine is concentrated in the human fetus, achieving an F:M concentration ratio of 1.32. Rodent studies revealed a possible 1048 reduction in implantation numbers and only minor skeletal abnormalities even when the dose approximated 400the MRHD. Stavudine readily crosses the rhesus macaque placenta.

Breastfeeding

There is no published experience in nursing women. It is unknown whether stavudine enters human breast milk. It is excreted into rodent milk. Breastfeeding is contraindicated in HIV-infected nursing women when formula is available to reduce the risk of neonatal transmission.

Pregnancy

. St. John?s wort is an herb used medicinally for centuries. The composition of St. John?s wort and how it might work are not well understood. It contains multiple bioactive substances. The naphthodianthrones hypericin and pseudohypericin and multiple flavonoids have generated interest as potential 1049 antidepressant and antiviral agents. In vitro studies reveal MAO inhibitory activity. Studies suggest that St. John?s wort is of no benefit in treating major depression of moderate severity. A National Institutes of Health study revealed that concomitant administration of St. John?s wort and indinavir substantially decreased indinavir plasma concentrations, potentially due to induction of CYP3A4 by St. John?s wort. There are no adequate reports or well-controlled studies of St. John?s wort during pregnancy. Relevant questions remain regarding the use of St. John?s wort in HIV-positive pregnant women treated concomitantly with protease inhibitors and NNTRIs. St. John?s wort is best avoided during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether St. John?s wort crosses the human placenta. One rodent study suggests maternal administration before and throughout gestation does not affect long-term growth and physical maturation of the exposed offspring.

Breastfeeding

There are no adequate reports or well-controlled studies of St. John?s wort in Breastfeeding women. One observational study suggests an increased prevalence of neonatal drowsiness/lethargy compared to control. Another study noted that hyperforin was excreted into breast milk at low levels, but was at or below the level of detection in the neonates (n = 2). M:P ratios ranged from 0.04 to 0.13. The relative infant dose of 0.9-2.5% indicates that infant exposure to hyperforin through milk is comparable to levels reported in most studies assessing antidepressants or neuroleptics. No

Pregnancy

. Streptokinase is a purified bacterial protein produced by group C b-hemolytic streptococci. There is no residual thrombotic material in 60-75% of patients treated with streptokinase vs. only 10% of those treated with heparin. Therapy preserves venous valve function in most cases, avoiding the pathologic changes that cause postphlebitic syndrome, which follows in 90% of the DVT patients treated with heparin alone. There are no adequate reports or well-controlled studies of streptokinase in pregnant women, though numerous case reports suggest relative safety compared to therapeutic alternatives. Of special note is its success with thrombotic mechanical mitral valves. Hemorrhage complicates <10% but may be severe. Because of the increased likelihood of resistance due to anti-streptokinase antibody, streptokinase may be ineffective within 1y of prior administration, or a streptococcal infection, such as streptococcal pharyngitis, acute rheumatic fever, or acute glomerulonephritis secondary to a streptococcal infection.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether streptokinase crosses the human placenta. The published case reports provide some reassurance. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There is no published experience in nursing women. It is unknown whether streptokinase enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of succinylcholine in pregnant women. It is the drug routinely used in rapid-sequence induction of general anesthesia to facilitate tracheal intubation for cesarean delivery. The large clinical experience is reassuring. Plasma cholinesterase levels decrease by1=4 during

Pregnancy

and for several days postpartum. Thus, a higher proportion of patients may experience prolonged apnea in response to succinylcholine when pregnant compared to nonpregnant.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Small amounts of succinylcholine are known to cross the placenta, but under normal conditions the amount of drug does not endanger the fetus. But because the amount that crosses depends on the M:F concentration gradient, apnea and 1052 flaccidity can occur in the neonate after repeated high doses, or in the presence of atypical maternal plasma cholinesterase. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether succinylcholine enters human breast milk. However, considering the indication and dosing, one-time succinylcholine use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. GERD poses a special challenge in pregnancy. Lifestyle and dietary modifications, change in sleeping posture, and antacid 1053 medications are the first lines of therapy. When these interventions are unsuccessful, sucralfate should be next. Therapy with H2receptor antagonists or proton pump inhibitors are generally reserved for women with refractory symptoms. There are no adequate reports or well-controlled studies of sucralfate in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies of sucralfate in human fetuses. It is only minimally absorbed across the GI tract, and thus should pose no risk to the fetus. Rodent studies are reassuring.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. While it is unknown whether sucralfate enters human breast milk, it is only minimally absorbed across the GI tract and should pose no risk to the Breastfeeding neonate.

Pregnancy

. Sufentanil is a potent opioid. When used in balanced general anesthesia, sufentanil has perhaps 10the potency of fentanyl. 1054 It is popular combined with a local anesthetic for a variety of neuraxial anesthetic techniques during labor. However, when choosing between fentanyl and sufentanil, sufentanil costs more and has a greater risk of dosing error because of its higher potency. The duration of analgesia is reduced in cocaine-abusing women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Sufentanil crosses the human placenta, achieving an F:M ratio of unity. Because of its low initial umbilical vein concentration, sufentanil may be the opioid of choice when delivery is imminent (<45min). Fetal acidosis increases placental transfer. It is used for fetal analgesia during a variety of procedures. Rodent studies are generally reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity does occur at doses twice the MRHD.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. However, considering the indication and dosing, one-time sufentanil use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. There is no published experience with sulconazole during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether sulconazole crosses the human placenta. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity was noted at doses 100the MRHD.

Breastfeeding

There is no published experience with sulconazole in nursing women. However, considering the dose and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. Toxoplasmosis is one of the most common parasitic infections in humans. There are no adequate reports or well-controlled studies of sulfadiazine in pregnant women for maternal disease. Sulfadiazine is also marketed as a silver-based cream used as an adjunct for the prevention and treatment of wound sepsis in patients with 2nd and 3rd degree burns.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Sulfadiazine crosses the human placenta and is used as a treatment for fetal toxoplasmosis in combination with pyrimethamine. Controversy continues as to how effective it is in preventing disease transmission. Since it is effective in the rhesus monkey model, treatment delay may explain the controversy. Rodent teratogenicity studies have not been performed. Other sulfonamides given at multiples of the MRHD are associated with cleft palate and bony abnormalities. It is also standard postnatally for the treatment of congenital toxoplasmosis. The extensive human experience associated with congenital toxoplasmosis is reassuring. There is no published experience to suggest any increase in the risk of kernicterus.

Breastfeeding

There is no published experience in nursing women. While it is unknown whether sulfadiazine enters human breast milk, it is excreted into cows? milk. There are no adverse effects published in breastfed children.

Pregnancy

. There are no adequate reports or well-controlled studies of sulfamethoxazole in pregnant women. When combined with trimethoprim, it is effective for the treatment of Q fever and for the treatment/prophylaxis of PCP. Trimethoprim- sulfamethoxazole is an alternative to high-dose penicillin for the treatment of listeriosis. It is also used to treat cystitis, but there are growing rates of bacterial resistance. 1058

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Sulfamethoxazole readily crosses the human placenta. One study noted a small increase in the rate of CV malformations after treatment with trimethoprim- sulfamethoxazole in the 2nd and 3rd trimesters. The causative agent was unclear. There is no published evidence to suggest it is associated with bilirubin toxicity, as is sulfisoxazole. Rodent studies performed at high multiples of the MRHD revealed an increased prevalence of cleft palate. It is probably best to avoid during the 1st trimester as it is an inhibitor of folate synthesis.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether sulfamethoxazole enters human breast milk.

Pregnancy

. Bacteria in the gut metabolize sulfasalazine to 5-aminosalicylic acid and sulfapyridine in a fashion unaffected by gender. There are no adequate reports or well-controlled studies of sulfasalazine in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Sulfasalazine and sulfapyridine cross the placenta with the M:F concentration ratios reaching unity. Large epidemiologic studies identify no evidence for human teratogenicity or an increased prevalence of adverse outcomes. Rodent studies are also reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Insignificant amounts of uncleaved sulfasalazine and 5-aminosalicylic acid are found in human milk; sulfapyridine levels are 30-60% of maternal serum. Sulfapyridine has poor bilirubin-displacing capacity.

Pregnancy

. There are no adequate reports or well-controlled studies of sulfisoxazole in pregnant women. Sulfisoxazole is an alternative to ampicillin, which some feel should no longer be used in the treatment of asymptomatic bacteriuria because of high rates of resistance. It has been used as an alternative for the treatment of chlamydia in erythromycin-allergic women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether sulfisoxazole crosses the human placenta. A large human experience is reassuring as there are no reports suggesting teratogenicity. Rodent studies performed at multiples of the MRHD were associated with cleft palate and bony abnormalities.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only small amounts of sulfisoxazole enter human breast milk, and it is generally considered compatible with breastfeeding.

Pregnancy

. Sulindac is an NSAID, also possessing analgesic and antipyretic activities. It also inhibits certain transcription factors such as NF- kB and AP-1, as does ibuprofen but not indomethacin. There are no adequate reports or well-controlled studies of sulindac in pregnant women. Very limited study suggests it is equally effective as indomethacin for the prolongation of

Pregnancy

in women with preterm labor. The use of sulindac until 34w after successful tocolysis fails to reduce the incidence of readmission for preterm labor or prolong the gestational age at delivery. It has also been used prophylactically in monochorionic twin pregnancies to reduce the volume of AF and stabilize the fetal lie.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Sulindac crosses the human placenta, producing F:M ratios approximating 0.4. Fetal levels are dependent on the maternal, as NSAID agents are not metabolized by the fetal kidney. Like other NSAIDs, sulindac causes dose-dependent and reversible ductal constriction and oligohydramnios. Rodent studies reveal an increased incidence of cleft palate (not seen with indomethacin), and there is an increased risk of IUGR and fetal death. 1062

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether sulindac enters human breast milk; it does enter rat milk.

Pregnancy

. There are no adequate reports or well-controlled studies of sumatriptan in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Only a small amount of sumatriptan (<5%) crosses the human placenta by passive transport, and should pose minimal risk to the fetus. Metabolites do not cross. Epidemiologic studies are reassuring. Rodent studies conducted at doses at least 6the MRHD revealed embryotoxicity and vascular and skeletal abnormalities. No adverse effects were noted at lower doses.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. A small amount of sumatriptan enters human breast milk, but the quantity absorbed by the neonate will be negligible.

Pregnancy

. Tacrine presumably elevates ACh in the cerebral cortex by slowing the degradation of ACh released by still-intact cholinergic neurons. It also appears to reduce excitatory amino acid toxicity. There is no evidence it alters the underlying dementia process. Plasma concentrations are 50% higher in women than men. There are no adequate reports or well-controlled studies of tacrine in pregnant women. The published literature is limited to two case reports 3 decades ago when it was used as a general anesthetic adjunct during cesarean delivery.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tacrine crosses the human placenta. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There is no published experience in nursing women. It is unknown whether tacrine enters human breast milk.

Pregnancy

. A growing number of obstetric patients have benefited from organ transplantation.

Pregnancy

is considered reasonable if the patient is 2y post transplantation, has good renal function without proteinuria, no uncontrolled arterial hypertension, and no evidence of ongoing rejection. However, these women are at high risk for an adverse outcome and should be followed at a tertiary care hospital. There are no adequate reports or well- controlled studies of tacrolimus in pregnant women. Though it has been used widely during

Pregnancy

without obvious adverse effect, the published experience is limited to case series. Clearance is not significantly altered.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses, and little animal experience. It is unknown whether tacrolimus crosses the placenta. Human studies do not reveal obvious evidence of teratogenicity. Immunosuppression is a theoretic concern.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Tacrolimus does enter human breast milk but at a very low concentration (<2ng/ml) with an M:P ratio <0.55. Using this information, the estimated dose ingested by a neonate would be <1mg/kg/d. Considering the low bioavailability of tacrolimus (<32%), the amount absorbed would be even lower (0.02-0.5% of the mother?s weight-adjusted dose).

Pregnancy

. Tamoxifen is one of four SERMs marketed in the US. The effect of SERMs on the estrogen receptor is tissue-dependent. It is an antagonist in the breast. The potential role of tamoxifen in the prevention of breast cancer is unclear and the subject of several large ongoing trials. It appears to reduce the incidence of ER+ invasive and noninvasive cancer. Until the completion of these trials, prophylaxis should probably be confined to women at high risk. Tamoxifen is an agonist in the uterus, increasing the risk of endometrial cancer and sarcoma. It is associated with an increased risk of thromboembolic disease. Tamoxifen does not cause infertility. Rather, it appears equal to clomiphene for ovulation induction in anovulatory women. There are no adequate reports or well-controlled studies of tamoxifen in pregnant women. Breast cancers diagnosed during

Pregnancy

and lactation typically are aggressive and present at an advanced stage. All women should be counseled on fertility preservation options. The timing of treatment modalities in pregnant women is complex and requires multidisciplinary input. Alternatives that are relatively safe for both mother and fetus are available, though unforeseen risks may exist. The published literature includes numerous cases of breast cancer diagnosed during pregnancy, with surgery followed by tamoxifen therapy usually after the 1st trimester. There were no obvious drug-related complications. The addition of tamoxifen to a regimen of misoprostol for medical abortion is unnecessary.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tamoxifen crosses the human placenta. Tamoxifen has effects on genital tract development similar to estrogen. There are several reports suggesting an association between 1st trimester exposure and craniofacial abnormalities. In rodents, tamoxifen inhibits uteroplacental artery dilation, decreases placental and fetal weights, and as a consequence increases the risk of fetal death.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether tamoxifen enters human breast milk. It is generally recommended women not breastfeed while taking tamoxifen.

Pregnancy

. There is no published experience with tazarotene during pregnancy. The maternal systemic concentration is reportedly low.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tazarotene crosses the human placenta. The maternal systemic concentration is reportedly low, and unpublished rodent teratogenicity studies reputedly are reassuring. Other drugs in this group are potent teratogens in mammals. Rodents treated topically with doses approximating 20% of the surface area have a greater risk of embryo loss and fetal malformation, including neural tube and cardiac anomalies.

Breastfeeding

There is no published experience in nursing women. It is unknown whether tazarotene enters human breast milk. It is excreted into rodent milk. However, considering the dose and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. Technetium-99m decays by isomeric transition with a t/2 of 6h. Its clearance is reduced in women. There are no adequate reports or well-controlled studies of technetium-99m in pregnant women. There is a long clinical experience that supports its use during

Pregnancy

when medically indicated. A diagnostically indicated test should not be withheld because of pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Technetium-99m crosses the human placenta, but delivers a maximal total fetal dose of <5mGy, far below the 50mGy considered the threshold for concern. Rodent teratogenicity studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Technetium-99m is excreted in human milk during lactation for about 24h after administration. While formula feedings for at least 24h after testing may seem prudent, a single case report suggests this may not be necessary. In this instance, sample radioactivity concentration peaked at 15h and decayed monoexponentially (half-clearance time was 4.8h). The estimated effective dose to the infant from ingestion alone was approximately 0.02mSv, suggesting interruption of Breastfeeding may not be necessary during early lactation.

Pregnancy

. There are no published reports of tegaserod use during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tegaserod crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. Tegaserod enters human breast milk with a high M:P ratio. Its impact on the neonate is unknown.

Pregnancy

. The plasma concentration of telmisartan is 2-3higher in females than in males. There is no published experience with telmisartan during pregnancy. Inhibitors of the renin-angiotensin system should be avoided during

Pregnancy

for fetal indications. The lowest effective dose should be used when telmisartan is required during

Pregnancy

for BP control.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether telmisartan crosses the human placenta. Inhibitors of the renin-angiotensin system are considered contraindicated throughout

Pregnancy

as their use has been associated with cranial hypoplasia, anuria, reversible or irreversible renal failure, death, oligohydramnios, prematurity, IUGR, and PDA. If oligohydramnios is observed, telmisartan should be discontinued unless considered lifesaving for the mother. Antenatal surveillance (e.g., BPP) may be appropriate, depending upon gestational age. Oligohydramnios may not appear until after irreversible injury. There is a single report of neonatal renal failure after antenatal exposure. Neonates exposed should be closely observed for hypotension, oliguria, and hyperkalemia. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether telmisartan enters human breast milk. It is excreted into rodent milk.

Pregnancy

. Residual medication effects (??hangover??) are essentially absent with temazepam, and early morning awakening, a particular problem for the geriatric patient, is significantly reduced compared to similar agents. REM sleep is unchanged. There are no adequate reports or well-controlled studies of temazepam in pregnant women. One case report suggested an association with a fetal demise.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Temazepam crosses the 2nd trimester human placenta, achieving an F:M ratio approximating 0.38 1h after 10mg IV. The ratio was stable between 60 and 120min, but rose with advancing gestation age. Third trimester studies are unavailable. Several studies suggest an increased prevalence of fetal malformation after diazepam use during the 1st trimester. Decreased fetal movement frequently follows IV diazepam administration, and prolonged CNS depression may occur in neonates due to their inability to metabolize. It is unknown whether the effect of temazepam is similar. The shortest course and the lowest dose should be used if indicated during pregnancy. Rodent teratogenicity studies reveal an increased prevalence of skeletal abnormalities and embryo loss.

Breastfeeding

Tenazepam is excreted into breast milk. In the one report, at concentrations of 26-28mcg/L for the pre- and postfeed samples, the M:P ratio for temazepam ranged from <0.09 to <0.63 (mean <0.18). Benzodiazepines in general enter human breast milk and may cause lethargy, sedation, and weight loss in infants. Some newborns exposed antenatally to diazepam exhibit either the floppy infant syndrome, or marked neonatal withdrawal symptoms. 1074

Pregnancy

. There is no published experience with temozolomide during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether temozolomide crosses the human placenta. Rodent teratogenicity studies reveal an increased prevalence of multiple malformations.

Breastfeeding

There is no published experience in nursing women. It is unknown whether temozolomide enters human breast milk.

Pregnancy

. The published experience with tenecteplase during

Pregnancy

is limited to case reports including one in the first trimester.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tenecteplase crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity occurs with high doses.

Breastfeeding

There is no published experience in nursing women. It is unknown whether tenecteplase enters human breast milk.

Pregnancy

. There are few well-controlled studies of tenofovir in pregnant women. Intrapartum and neonatal single-dose nevirapine are essential components in the prevention of perinatal HIV in resource-constrained settings, but can induce resistance to NNRTIs. Recently, it was found that a single dose of tenofovir and emtricitabine at delivery reduced resistance to NNRTIs at 6w after delivery by half. The clearance of some NRTIs is increased during pregnancy. There are no data describing the effect of

Pregnancy

on the pharmacokinetics of tenofovir.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tenofovir crosses the human placenta. Small case series are to date reassuring. Tenofovir crosses the rhesus monkey placenta sufficiently well to lower the fetal viral load. In doing so, there is a transient delay in bone growth that may be IGF-I mediated. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether tenofovir enters human breast milk. However, it is excreted into macaque and rodent milk. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. There is no published experience with terazosin during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether terazosin crosses the human placenta. While rodent studies are generally reassuring, revealing no evidence of teratogenicity, embryotoxicity and IUGR were noted after doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether terazosin enters human breast milk. 1078

Pregnancy

. There is no published experience with terbinafine during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether terbinafine crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. The manufacturer reports terbinafine achieves an M:P ratio of 7:1 after oral administration. Until data to the contrary becone available, Breastfeeding should be avoided.

Pregnancy

. Terbutaline is a popular and effective agent for the treatment of asthma during pregnancy. While generally considered a selective b2-agonist based on in vitro study, its clinical profile is less specific. As with all other b-mimetics and most tocolytic agents, terbutaline is associated with an ?48h delay in delivery compared to placebo in women with preterm labor.

Pregnancy

outcome is altered only when coupled with antenatal steroid administration. As it is for all other currently available drugs, the use of either oral or continuous SC treatment is ineffective preterm labor prophylaxis. Maternal Side effects include pulmonary edema, hypotension, tachycardia, palpitations, arrhythmia, nervousness, tremor, headache, N/V, drowsiness, sweating, muscle cramps, and hyperglycemia.

Fetal Health

Terbutaline crosses the human placenta, achieving an F:M ratio between 0.11 and 0.48 after a single IV dose immediately prior to elective cesarean delivery. Levels approach unity after several hours. Multiple case reports suggest it is chronotropic in fetuses with complete heart block. The effect, if any, is often transient perhaps because b-adrenergic innervation is still relatively immature even at birth. Allegations that terbutaline exposure during

Pregnancy

causes autism cannot be sustained on any level because of the high doses studied coupled to a lack of evidence that terbutaline crosses the fetal blood-brain barrier. Paradoxically, there is no receptor desensitization demonstrable in the fetal rat heart exposed chronically to terbutaline. Rodent studies are reassuring, showing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Terbutaline increases the frequency of fetal breathing. Chronic terbutaline exposure increases cardiac size and HR in fetal guinea pigs. Overall, it appears long-term terbutaline use has measurable fetal affects at least in rodents. Breastfeeding Terbutaline is excreted into human breast milk, reaching M:P ratios in excess of 2. Yet, the amount ingested is <1% of the maternal dose, and the neonatal level undetectable.

Pregnancy

. Terconazole is a member of a series of imidazoles whose effectiveness appears similar. There are no adequate reports or well-controlled studies of terconazole in pregnant women. Topical imidazole appears to be more effective than nystatin for treating symptomatic vaginal candidiasis in pregnancy. Treatment periods of 7d may be necessary during

Pregnancy

rather than the shorter courses typically recommended.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether terconazole crosses the human placenta. Rodent studies are generally reassuring, revealing 1082 no evidence of teratogenicity or IUGR until the dose exceeds 20the MRHD, when skeletal abnormalities and embryotoxicity are noted. The no-effect oral dose (10mg/kg/d) produces a mean peak plasma level in pregnant rats 44the mean peak plasma levels seen after intravaginal administration.

Breastfeeding

There is no published experience in nursing women. It is unknown whether terconazole enters human breast milk.

Pregnancy

. Tetanus immune globulin creates passive immunity to the toxin of C. tetani. Naturally acquired immunity to tetanus toxin is rare in the US. Universal primary vaccination, with subsequent timed boosters to maintain adequate antitoxin levels, is required for all age groups. There are no adequate reports or well-controlled studies of tetanus immune globulin in pregnant women. Tetanus is a highly lethal disease and a significant cause of maternal death in some locales. It appears the antibodies produced in response to tetanus toxoid during

Pregnancy

have low protective capacity, strengthening the importance of tetanus immune globulin prophylaxis during pregnancy. The long clinical experience suggests safety. 1083

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Tetanus immune globulin crosses the human placenta and provides at least partial coverage for the neonate. Maternal immunization does not interfere with neonatal response to the DPT series. The degree of IgG transfer is lower in the preterm compared to the term neonate, and there appears to be a maximal transfer rate. Rodent teratogenicity studies have not been performed, but there is no reason to hypothesize the antibody may damage the fetus.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether tetanus immune globulin enters human breast milk. However, the long clinical experience in humans is reassuring. It does enter the colostrum of horses and actually can reduce the foal?s response to vaccination.

Pregnancy

. Serologic tests demonstrate naturally acquired immunity to tetanus toxin is rare in the US. Universal primary vaccination, with subsequent timed boosters to maintain adequate antitoxin levels, is required for all age groups. Tetanus is a highly lethal disease and a significant cause of maternal death in some locales. Tetanus toxoid is a highly effective antigen; a completed primary series generally induces protection that persists ?10 years. Increasing the interval between primary immunizing doses to 6mo or longer does not interfere with the final immunity. Any dose of tetanus toxoid received, even a decade earlier, is counted as the first immunizing injection. There are no adequate reports or well-controlled studies of tetanus toxoid in pregnant women. Pregnant women do respond. In many geographic locales, a cogent argument can be made for routine immunization with at least 1 dose during

Pregnancy

to protect both mother and newborn.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. The antibodies generated in response to tetanus toxoid appear to cross the human placenta, and are capable of stimulating active immunity in the term fetus. The long clinical experience with immunization during

Pregnancy

is reassuring. Maternal immunization protects against neonatal tetanus and should be public policy in many geographic locales.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether tetanus toxoid enters human breast milk.

Pregnancy

. Tetracaine produces 2-3h of surgical anesthesia depending on the site of surgery (i.e., intra-abdominal vs. lower limb/perineal). The extent and degree of anesthesia depend on dose, specific gravity of the anesthetic solution, volume used, and the position of the patient during and immediately after injection. There are no adequate reports or well-controlled studies of tetracaine in pregnant women. Although once routinely used (mixed with either 10% glucose or 10% procaine) for spinal anesthesia for cesarean delivery, tetracaine has been supplanted by bupivacaine as the spinal agent of choice for cesarean delivery.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tetracaine crosses the human placenta. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether tetracaine enters human breast milk. Other local anesthetics are excreted. Considering the indication and dosing, one-time tetracaine use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Tetracycline is a broad-spectrum antibiotic prepared from certain Streptomyces species. When penicillin is contraindicated, tetracycline-class agents are alternatives for the treatment of gonorrhea (1.5g PO, then 0.5g qid for a total of 9.0g), syphilis and yaws, Listeria monocytogenes, Clostridium species, B. anthracis, Fusobacterium fusiforme (Vincent?s infection), and Actinomyces species. Tetracycline may be more hepatotoxic than doxycycline. There are no adequate reports or well-controlled studies of tetracycline in pregnant women. It is generally avoided during

Pregnancy

because of fetal considerations.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Tetracycline crosses the human placenta and may cause a yellow-gray-brown tooth discoloration in adults after fetal/childhood exposure. It is unlikely topically applied tetracycline achieves a clinically relevant systemic level. Another tetracycline, oxytetracycline (but not doxycycline) is associated with an increased risk of NTDs, cleft palate, and CV defects. There are no similar studies for tetracycline. Rodent studies are otherwise generally reassuring, revealing no evidence of teratogenicity, but some embryotoxicity at high doses.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Tetracycline enters human breast milk, though the kinetics remain to be elucidated. Clinical experience suggests that maternal oral ingestion is compatible with breastfeeding.

Pregnancy

. Thalidomide is a known human teratogen and contraindicated during pregnancy. It is also excreted in semen, and treated males should wear a condom during coitus. Initially banned in the US, it has proven a superb drug for the treatment of several formerly resistant diseases. Its potential indications are growing, increasing the likelihood of an inadvertent pregnancy. Effective contraception is mandatory. While there are no reports of thalidomide-related birth defects in the US since its return to the market, there are scattered reports elsewhere, providing a constant reminder to providers. There are no adequate reports or well-controlled studies of thalidomide in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Thalidomide crosses the human placenta and is a potent human (but not rodent) teratogen, causing limb abnormalities after 1st trimester exposure, perhaps by creating a pro-oxidant balance. Even a single 50mg dose can cause defects. If

Pregnancy

occurs, the drug should be discontinued and the patient referred to a fetal medicine expert for evaluation and counseling. Any suspected fetal exposure to thalidomide must be reported to the FDA via the MedWatch program at 1-800-FDA-1088 and also to the Celgene Corporation. It is of note that recent cases of thalidomide embryopathy result from sharing medication and were not detected by normal surveillance procedures.

Breastfeeding

There is no published experience in nursing women. It is unknown whether thalidomide enters human breast milk.

Pregnancy

. Theophylline has two distinct actions on the airways of women with reversible airway obstruction: bronchodilation and nonbronchodilator prophylactic effects. Although 1% of pregnant women have asthma, it is often underrecognized and suboptimally treated. Severe, uncontrolled asthma increases the likelihood of maternal and fetal morbidity and death. Pharmacologic therapy is often necessary during pregnancy. Women with well-controlled asthma during

Pregnancy

have outcomes as good as those of their nonasthmatic peers. Its clearance of theophylline is altered little during either the 1st and 2nd trimesters, but significantly decreased in the 3rd trimester and puerperium. Benefit:risk considerations suggest inhaled asthma medications such as b-mimetics and corticosteroids are first-line agents, with theophylline a second-line agent for the treatment of asthma during pregnancy. The risk of exacerbation is high immediately postpartum, but overall severity usually reverts to preconception levels postpartum. Asthma tends to follow a similar course in subsequent pregnancies.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Theophylline crosses the human placenta, reaching an F:M ratio of unity in a brief time. It dilates in vitro constricted placental arteries. While the limited rat teratogen studies are reassuring, theophylline producing more than 5the recommended human therapeutic concentration causes fetal toxicity, cleft palate, and skeletal malformations in rabbits. In the chick (a poor model for humans), theophylline is associated with an increased prevalence of CV malformations.

Breastfeeding

Theophylline enters human breast milk, achieving an M:P ratio between 0.6 and 0.9. It can cause irritability in the nursing newborn, presumably because of the long neonatal t/2. Neonatal toxicity is unlikely. Women who choose to breastfeed should monitor their children?s behavior closely.

Pregnancy

. Thiabendazole is usually a second-line therapy for pinworm behind piperazine. However, when enterobiasis occurs, additional therapy is not required for most patients. Thiabendazole should be used for the following only when more specific therapy is unavailable or cannot be used or when further therapy with a second agent is desirable: uncinariasis (hookworm: Necator americanus and Ancylostoma duodenale); trichuriasis (whipworm); ascariasis (large roundworm). There are no adequate reports or well-controlled studies of thiabendazole in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether thiabendazole crosses the human placenta. It crosses the rodent placenta, though the kinetics remain to be elucidated. Rodent teratogen studies are inconsistent, revealing skeletal and cleft palate abnormalities at 10the MRHD in only some investigations. These adverse effects are now thought likely the product of maternal toxicity.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether thiabendazole enters human breast milk.

Pregnancy

. Pure thiamine deficiency is rare. Multiple vitamin deficiencies should be suspected in any case of dietary inadequacy. There are no adequate reports or well-controlled studies of thiamine in pregnant women. Despite its inclusion in prenatal vitamins, thiamine deficiency is not uncommon during pregnancy. Wernicke?s encephalopathy is reported during pregnancy, often in association with hyperemesis. When given as part of a multivitamin prenatal supplement, thiamine improves weight gain among HIV-infected women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Thiamine is actively transported across the human placenta, reaching an F:M ratio of 10. Thus, maternal supplementation is unlikely to alter the fetal thiamine to any clinically relevant extent.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Thiamine enters human breast milk, and maternal supplementation increases milk content. The thiamine content in milk from unsupplemented women is considered inadequate for requirements of the neonate. 1094

Pregnancy

. There are no adequate reports or well-controlled studies of thioguanine in pregnant women. The published literature includes only case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is likely thioguanine crosses the human placenta, but in low concentration. In one case report, the 6-thioguanine nucleotide level was significantly lower in the erythrocytes of the infant compared to the mother (ratio 1:12). While most of the reported cases end with a normal outcome, few women receive monotherapy. It is possible thioguanine is at least a modest teratogen in humans. Thioguanine is teratogenic in rats at 5the MRHD, causing embryotoxicity and an increased prevalence of cranial defects, general skeletal hypoplasia, hydrocephalus, ventral hernia, situs inversus, incomplete limb development, and IUGR.

Breastfeeding

There is no published experience in nursing women. It is unknown whether thioguanine enters human breast milk. However, the thioguanine metabolite of azathioprine apparently does not enter breast milk to a detectable level. 1095

Pregnancy

. Thiopental is an ultra-short-acting CNS depressant in use for more than 60y. It induces hypnosis and anesthesia, but not analgesia. Recovery after a small dose is rapid, with some somnolence and retrograde amnesia. Repeated IV doses lead to prolonged anesthesia because the fatty tissues act as a reservoir. There are no adequate reports or well-controlled studies of thiopental in pregnant women. It remains a popular agent for rapid-sequence induction of general anesthesia for cesarean section. Hypotension and awareness are more common when it is used for induction than when ketamine is used.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Thiopental rapidly crosses the human placenta, achieving an F:M ratio approximating 0.8 within 5min of maternal IV administration. However, the long clinical history of use in pregnant women is reassuring. Peak levels occur in the fetal rat in 10min. In the fetal sheep, thiopental reduces cerebral blood flow and oxygen delivery, suggesting it should be avoided during a delivery for fetal distress. Rodent teratogen studies have not been performed. Thiopental is a teratogen in the chick embryo, increasing the prevalence of CNS malformations.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Thiopental enters human breast milk, but the concentrations are negligible by 36h postoperatively.

Pregnancy

. There are no adequate reports or well-controlled studies of thioridazine in pregnant women. The published literature is confined to case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether thioridazine crosses the human placenta.

Breastfeeding

There is no published experience in nursing women. It is unknown whether thioridazine enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of thiothixene in pregnant women. The published literature consists of a single case report.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether thiothixene crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether thiothixene enters human breast milk.

Pregnancy

. Tiagabine is a 2nd-generation anticonvulsant frequently employed as adjunct therapy. It is not an enzyme inducer, and there is no interaction between tiagabine and oral contraceptive agents. There are no adequate reports or well-controlled studies of tiagabine in pregnant women. No systematic information is available on the pharmacokinetics during pregnancy. Caution dictates maternal levels be measured periodically.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tiagabine crosses the human placenta. Tiagabine is a rodent teratogen, increasing the prevalence of craniofacial, appendicular, and visceral defects in addition to IUGR.

Breastfeeding

There is no published experience in nursing women. It is unknown whether tiagabine enters human breast milk. It is excreted in rodent milk.

Pregnancy

. Ticarcillin is an extended-spectrum penicillin. It is primarily indicated for gram-negative infections and is often combined with an aminoglycoside. Clavulanic acid is a b-lactam that inactivates a wide range of b-lactamase enzymes commonly found in microorganisms resistant to penicillins and cephalosporins. The combination of ticarcillin-clavulanate has a microbiologic spectrum similar to gentamicin and clindamycin. There are no adequate reports or well-controlled studies of ticarcillin in pregnant women. Like other antibiotics, it reduces the risk of postpartum endomyometritis in women with PPROM, but may increase the proportion of neonates with sepsis secondary to ampicillin-resistant organisms.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Transfer of ticarcillin across the human placenta is slow, 1100 but it does accumulate in the fetal compartment over time. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Ticarcillin enters human breast milk. However, the quantity (2-2.5mg/L) is too low to have clinical relevance.

Pregnancy

. Ticlopidine potentiates the effect of aspirin or other NSAIDs on platelet aggregation. There are no adequate reports or well-controlled studies of ticlopidine in pregnant women. The published experience is limited to case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether ticlopidine crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. 1101

Breastfeeding

There is no published experience in nursing women. It is unknown whether ticlopidine enters human breast milk. It is excreted into rodent milk.

Pregnancy

. There are no adequate reports or well-controlled studies of timolol in pregnant women. Timolol is superior to a-methyldopa for the treatment of puerperal hypertension. It is unclear whether timolol offers any therapeutic advantage over another b-blocker. There are only case reports of its use to treat glaucoma.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Timolol crosses the isolated perfused human placenta, though the in vivo kinetics remain to be elucidated. It decreases the FHR after administration to the ewe. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Timolol is excreted into human milk, achieving an M:P ratio of 0.8 in one study, but higher in another. In one woman using eye drops, the milk concentration ranged from 0-0.4 ng/ml. The theoretic relative infant dose would be 0.024%.

Pregnancy

. Thromboembolic disease remains a major cause of

Pregnancy

morbidity and death. Tinzaparin is an LMWH extracted from pig. It is at least as effective as unfractionated heparin for the treatment and prevention of thromboembolic disease. Post-cesarean section, it reduces thrombin-antithrombin complex concentration more effectively than enoxaparin. It is unknown whether that enhancement means improved prophylaxis. Most anesthesiologists prefer to wait 24h after the last dose of tinzaparin (even if given 175U/kg qd) before induction of neuraxial anesthesia. Because the clearance of other LMWHs are increased by pregnancy, it is probably best to monitor anti-Xa activity at least once per trimester and administer the drug in 2 divided doses beginning with 250IU/kg qd. In support of this conclusion, one study noted that women receiving tinzaparin (50IU/kg) frequently had peak (4h) anti-Xa levels <0.1IU/ml and that 46% of these patients required dose adjustment. Likewise, anti-Xa activity was found to be low over the 24h period. A starting dose of 75IU/kg, once daily, gave greater anti-Xa cover over the 24h period. The findings suggest the pharmacokinetics of tinzaparin are affected by pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Tinzaparin does not cross the human placenta. Rodent studies are reassuring, revealing no evidence of 1104 teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether tinzaparin enters human breast milk.

Pregnancy

. Tizanidine is effective for the treatment of tension headache and the spasticity associated with MS. Sedation is common. There are no adequate reports or well-controlled studies in pregnant women. Retrospective analysis of population pharmacokinetic data after single- and multiple-dose administration of 4mg showed women taking oral contraceptives had 50% lower clearance compared to women not on oral contraceptives.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tizanidine crosses the 1105 human placenta. Rodent studies are predominantly reassuring, though the doses tested were only modest multiples of the MRHD. They reveal some evidence of prolonged

Pregnancy

and embryotoxicity.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether tizanidine enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of tobramycin in pregnant women. The clearance of tobramycin during

Pregnancy

and the puerperium is increased, requiring 3mg/kg or more to obtain adequate peak and trough levels.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tobramycin crosses the human placenta. Other aminoglycoside antibiotics do cross, and there are reports of total, irreversible, bilateral congenital deafness after streptomycin. Serious Side effects to mother, fetus, or newborn are not reported after treatment with other aminoglycosides. Tobramycin likely poses no greater risk than gentamicin to the fetus. Systemic levels are much lower after nebulizer or ophthalmic administration compared to parenteral route. In the rat, tobramycin accumulates in the placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. The highest doses caused excess maternal toxicity with increased fetal wastage. Breastfeeding There are no adequate reports or well-controlled studies in nursing women. Small amounts of tobramycin are excreted into human breast milk. Milk levels ranged from undetectable to 0.5mcg/ml in a study of 5 women treated with 80mg IM. As tobramycin is poorly absorbed orally, it is very unlikely the unsupplemented neonate would achieve a clinically relevant level.

Pregnancy

. Tocainide is similar to lidocaine. There is no published experience with tocainide during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tocainide crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity occurs at high doses with maternal toxicity.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Tocainide enters human breast milk, though the kinetics remain to be elucidated.

Pregnancy

. Diet remains the first-line treatment of diabetes mellitus type 2. Caloric restriction and weight loss are essential in the obese diabetic patient, and may alone be effective controlling blood glucose and symptoms. The importance of regular physical 1108 activity should be stressed, and CV risk factors identified and corrected if possible. When this approach fails, oral hypoglycemic agents may be indicated. Tolazamide is a first-generation sulfonylurea. Sulfonylureas may be associated with an excess of CV death. There are no adequate reports or well-controlled studies of tolazamide in pregnant women. Additional study is necessary. Other oral hypoglycemic agents (e.g., glyburide) are poorly transported across the placenta.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tolazamide crosses the human placenta. Prolonged, severe hypoglycemia (4-10d) has been reported in neonates delivered to women receiving a sulfonylurea at the time of delivery. This is most common with agents with a prolonged t/2. Tolazamide should be discontinued at least 2w before the EDC. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Only with the highest doses (>100the MRHD) was embryotoxicity noted.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether tolazamide enters human breast milk. Other sulfonylurea drugs are excreted into breast milk.

Pregnancy

. Diet remains the first-line treatment of diabetes mellitus type 2. Caloric restriction and weight loss are essential in the treatment of the obese diabetic patient, and may alone be effective in controlling blood glucose and symptoms. The importance of regular physical activity must also be stressed, and CV risk factors identified and corrected where possible. When this approach fails, oral hypoglycemic agents may be indicated. There are no adequate reports or well-controlled studies of tolbutamide in pregnant women. Efficient placental transport renders it a poor selection during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Tolbutamide crosses the human placenta relatively efficiently compared to glyburide. The fetal pancreas is responsive. Prolonged and severe hypoglycemia (4-10d) is reported in neonates born to mothers receiving a sulfonylurea at the time of delivery. This is more frequent with agents having a prolonged t/2. If tolbutamide is used during pregnancy, it should be discontinued at least 2w before the expected delivery date. Tolbutamide is teratogenic in rats, associated with an increased prevalence of ocular and bony abnormalities at doses 25-100? the MRHD. Similar studies in rabbits were negative.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Tolbutamide enters human breast milk, but the kinetics remain to be elucidated.

Pregnancy

. There are no adequate reports or well-controlled studies of tolmetin in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tolmetin crosses the human placenta. Rodent studies performed up to 1.5the MRHD were reassuring, revealing no evidence of teratogenicity. 1111 Some bone demineralization is seen at the highest doses. Other drugs in this class are known to cause constriction of the ductus arteriosus in utero. There is no reason to expect tolmetin is different.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Small quantities of tolmetin are excreted into human breast milk. Though the kinetics remain to be elucidated, the milk level was only 0.18mg/ml 40min after 400mg PO.

Pregnancy

. There is no published experience with tolterodine during pregnancy. There is also probably no indication for its use during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tolterodine crosses the human placenta. It crosses the rodent placenta, concentrating in the placenta and the fetal liver, brain, and spinal cord. Rodent studies conducted at doses 20-25the MRHD revealed 1112 embryotoxicity, IUGR, and birth defects, including cleft palate and skeletal malformations. In guinea pigs, maternal treatment decreases ACh-mediated relaxation of isolated aorta.

Breastfeeding

There is no published experience in nursing women. It is unknown whether tolterodine enters human breast milk. It is excreted at low levels into rodent milk, with neonates ingesting <0.5% of the dose.

Pregnancy

. Topiramate increases the metabolism of ethinyl estradiol and progestogens. If a women wishes to take OCPs, the preparation should contain at least 50mcg of ethinyl estradiol. Levonorgestrel implants are contraindicated because of the increased risk of contraceptive failure. Further, it is recommended that medroxyprogesterone injections be given q10w rather than q12w. There are no adequate reports or well-controlled studies of topiramate in pregnant women. Folate supplementation preconception is prudent. As for most psychotropic drugs, monotherapy and the lowest effective quantity given in divided doses to minimize the peaks may minimize the risks. Many recommend vitamin K (10mg PO qd) be given the last 4w of

Pregnancy

for women taking hepatic enzyme?inducing 1113 anticonvulsants such as topiramate. The scientific support for this practice is weak.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Topiramate readily crosses the human placenta, reaching F:M ratios approaching unity. There is too little human experience where topiramate is a teratogen in rodents. Preliminary after market data suggest an increase in major congenital malformations, especially oral clefts. There is a dose- dependent increase in the prevalence of craniofacial and limb malformations, and IUGR, even at doses a fraction of the MRHD.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Topiramate enters human breast milk at low concentrations; Breastfeeding neonates have levels around the lower limit of detection.

Pregnancy

. There is no published experience with torsemide during pregnancy. Diuretics should not be used for the treatment of physiologic edema of pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether torsemide crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether torsemide enters human breast milk.

Pregnancy

. Tramadol is a centrally acting analgesic. There are no adequate reports or well-controlled studies of tramadol in pregnant women. There are a few studies using it intrathecally. A single study comparing tramadol with meperidine for labor analgesia concluded it created less maternal sedation and fetal respiratory depression. Tramadol reduces postanesthetic shivering with a lower frequency of somnolence than meperidine. There is no evidence of a difference between meperidine and tramadol in terms of pain relief, interval to delivery, or instrumental or operative delivery. It is an excellent oral agent for the relief of significant postoperative pain. However, it is no better than ibuprofen for the treatment of postabortal pain. In fact, ibuprofen is somewhat more effective at reducing pain 30min after surgical abortion. 1116

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Tramadol crosses the human placenta, achieving an F:M ratio of 0.83 with the concentrations approaching unity. Chronic use during

Pregnancy

may lead to physical dependence and postpartum withdrawal symptoms in the newborn. Rodent studies are generally reassuring, revealing only embryo and maternal toxicity at high concentrations, and no teratogenicity or IUGR.

Breastfeeding

A small amount of tramadol enters human breast milk. The estimated relative infant dose of 2.88% is low.

Pregnancy

. There is no published experience with trandolapril during pregnancy. Agents that inhibit the renin-angiotensin system should be avoided during

Pregnancy

for fetal indications.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether trandolapril crosses the human placenta. Other drugs of this class do cross the placenta. Adverse fetal effects are reported from drugs that inhibit the renin-angiotensin system throughout pregnancy. Later exposure is associated with cranial hypoplasia, anuria, reversible or irreversible renal failure, death, oligohydramnios, prematurity, IUGR, and PDA. If oligohydramnios is observed, trandolapril should be discontinued unless considered lifesaving. Antenatal surveillance (e.g., BPP) may be appropriate, depending upon the week of pregnancy. Oligohydramnios may not appear until after the fetus has sustained irreversible injury. Neonates exposed in utero should be closely observed for hypotension, oliguria, and hyperkalemia. Rodent and primate studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether trandolapril enters human breast milk. It is excreted into rodent milk.

Pregnancy

. Depression is common during and after pregnancy, but typically goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. Tranylcypromine is best suited for patients who have failed to respond to drugs more commonly used for depression. There is no published experience with tranylcypromine during pregnancy. Its inhibition of PGI2 synthetase raises theoretic concerns.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tranylcypromine crosses the human placenta. It does cross the rat placenta, but rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether tranylcypromine enters human breast milk. It is excreted into rodent milk. As for most psychotropic drugs, monotherapy and the lowest effective quantity given in divided doses to minimize the peaks may minimize the risks.

Pregnancy

. Depression is common in reproductive-age women and frequently overlooked or minimized by the care provider. There is no reason a priori to deny indicated treatment during pregnancy. The published experience with trazodone during

Pregnancy

is limited but reassuring. In one report, levels were lower in the 1st and 2nd trimesters compared to the 3rd. The elimination t/2 was unchanged though.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether trazodone crosses the human placenta. Cohort studies are reassuring, revealing no increase in the prevalence of adverse outcomes. Trazodone crosses the rat placenta, and rodent teratogenicity studies reveal an increased risk of embryo absorption and malformations (rabbit) at doses that are multiples of the MRHD.

Breastfeeding

Trazodone enters human breast milk, but the amount ingested by the neonate is not clinically relevant.

Pregnancy

. Significant pulmonary hypertension is associated with a high maternal mortality rate during the peripartum. There is no published experience with treprostinil during pregnancy. 1121

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether treprostinil crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether treprostinil enters human breast milk.

Pregnancy

. Some retinoid agents can be highly toxic to the fetus. Within 7d of tretinoin therapy, a blood or urine

Pregnancy

test with a sensitivity of at least 50 mIU/L should be performed. When possible, tretinoin should be delayed until a negative result from this test is obtained. When a delay is not possible, the patient should be placed on two reliable forms of contraception.

Pregnancy

testing and contraception counseling should be repeated monthly throughout the period of tretinoin treatment. Tretinoin inhibits in vitro decidualization of endometrial stroma. There are no adequate reports or well-controlled studies of tretinoin in pregnant women. The published experience consists of case reports of acute promyelocytic leukemia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Tretinoin crosses the human placenta. Epidemiologic data are reassuring: 106 pregnant women with 1st trimester exposure to topical tretinoin were reported between 1983 and 2003 and prospectively followed. Birth outcomes were compared to 389 similarly followed women without exposure. There were no significant differences between groups in the proportion of pregnancies ending in spontaneous abortion, or infants with major structural defects. The groups were similar in gestation and size at birth. The prevalence of one or more retinoic acid?specific minor malformations did not differ between groups. Unfortunately, fewer than 10 neonates have been born to women treated with oral tretinoin during

Pregnancy

(virtually all after the 1st trimester) for acute promyelocytic leukemia. All had normal growth without apparent complications. Tretinoin is a teratogen in rodents and primates when given orally. Reported defects in these species include abnormalities of the CNS, musculoskeletal system, ear, eye, thymus, and great vessels; facial dysmorphia; cleft palate; and PTH deficiency. The offspring of diabetic mice are more prone to develop caudal regression after tretinoin exposure. The teratogenic effect of topically applied drug is less clear and is likely low if used as directed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether tretinoin enters human breast milk.

Pregnancy

. Triamcinolone is a fluorinated glucocorticoid. There are no adequate reports or well-controlled studies of triamcinolone in pregnant women. Triamcinolone appears to be at least as efficacious for the treatment of asthma during

Pregnancy

as beclomethasone. The suggestion that chronic topical application might lead to IUGR has yet to be confirmed by others. It is less likely the maternal systemic concentration will reach a clinically relevant level after either topical or inhalational use. In one study, PO triamcinolone caused a loss of circadian rhythms of cortisol, ACTH, estradiol, and unconjugated estriol, and modified the ultradian and circadian patterns of FHR. No differences in hormonal and biophysical parameters were found after the end of treatment, suggesting the inhibition of fetal and maternal adrenal glands modifies FHR patterns.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether triamcinolone crosses the human placenta. However, it does cross the nonhuman primate placenta and is relatively resistant to placental metabolism. The resulting F:M ratio approximates 0.6. Epidemiologic evidence is reassuring. Further, its administration to nonhuman primates at doses 5-60(10mg/kg) the MRHD increases the prevalence of IUGR and craniofacial defects. The extensive fetoplacental metabolism of cortisol to inactive metabolites and the resistance of triamcinolone to metabolic conversion result in greater triamcinolone than cortisol exposure. Triamcinolone also crosses the rodent placenta, and its fetal t/2 is significantly prolonged compared to cortisol. In several rodent models, triamcinolone causes cleft lip and palate, whereas cortisol does not. While there is no epidemiologic evidence suggesting PO triamcinolone is a teratogen in humans, prescribing caution especially during the 1st trimester seems prudent. It is less likely the maternal systemic concentration will reach a clinically relevant level after either topical or inhalational use.

Breastfeeding

There is no published experience in nursing women. It is unknown whether triamcinolone enters human breast milk. Topically applied drug likely poses little risk to the nursing newborn.

Pregnancy

. Triamterene has a unique mode of action. In addition to its diuretic effect, triamterene is also a folate antagonist. There are no adequate reports or well-controlled studies of triamterene in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Triamterene rapidly crosses the human placenta, reaching F:M levels approaching unity. Epidemiologic studies suggest that folate antagonists, including triamterene, may increase the risk not only of NTDs, but also of CV defects, oral 1126 clefts, and urinary tract defects. It crosses the rodent placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether triamterene enters human breast milk. It is excreted into rodent milk.

Pregnancy

. There are no adequate reports or well-controlled studies of triazolam in pregnant women. The published literature consists of scattered case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether triazolam crosses the human placenta. However, neonatal CNS depression has followed its use in the immediate antepartal period. Other benzodiazepines do cross the placenta, and in some rodent models, diazepam and chlordiazepoxide are associated with cleft lip and palate. Rodent teratogen studies have not been conducted.

Breastfeeding

There is no published experience in nursing women. It is unknown whether triazolam enters human breast milk. It is excreted in rodent milk.

Pregnancy

. Trifluoperazine has a number of effects, including the inhibition of calmodulin. There are no adequate reports or well-controlled studies of trifluoperazine in pregnant women. Trifluoperazine also has antiemetic properties similar to other phenothiazines. The published literature consists of scattered, typically uninformative case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Trifluoperazine apparently crosses the human placenta, but the kinetics remain to be elucidated. It is oxidized by human placental peroxidase. Calmodulin inhibition has the potential to adversely affect multiple developmentally important pathways. Rodent studies are generally reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Trifluoperazine enters human breast milk, but apparently at lower concentrations than haloperidol and chlorpromazine. As for most psychotropic drugs, monotherapy and the lowest effective quantity given in divided doses to minimize the peaks may minimize the risks.

Pregnancy

. There are no adequate reports or well-controlled studies of trimethobenzamide in pregnant women. It has been used for the treatment of morning sickness.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether trimethobenzamide crosses the human placenta. One epidemiologic study several decades old suggested an increased prevalence of major malformations. This observation has not been supported by subsequent study. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity occurred in several animals treated at 50-60the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether trimethobenzamide enters human breast milk.

Pregnancy

. Bacteriuria, with or without clinical symptoms, is common during pregnancy. If left untreated, 20-30% of patients develop acute pyelonephritis, which increases the risk of preterm labor and low-birth-weight infants. Established first-line drugs such as amoxicillin, ampicillin, and trimethoprim-sulfamethoxazole are associated with a high degree of resistance in E. coli, the most common pathogen in the urinary tract. Some 3-4% of women reportedly ingest trimethoprim during their pregnacy. Nitrofurantoin or a b-lactam agent are also first-line agents for the treatment of asymptomatic bacteriuria. The most powerful study to date documents an increased prevalence of placenta- mediated adverse events when trimethoprim is given: preeclampsia, severe preeclampsia, placental abruption, IUGR, and fetal death. A growing number of women are being treated with trimethoprim in combination of an array of antivirals for HIV-related complications. The impacts of these combinations are poorly studied. Trimethoprim-sulfamethoxazole is used for the treatment of Q fever during pregnancy. Women who develop Q fever should be treated for the duration of pregnancy, specifically if infected during the 1st trimester.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Transfer of trimethoprim across the human placenta 1131 is limited. The combination of trimethoprim-sulfamethoxazole has been associated with an increased risk of IUGR, CV, NTD, and urinary tract malformations. While there is no solid evidence solo therapy with trimethoprim is a human teratogen, the possibility it is a weak human teratogen cannot be excluded. Trimethoprim is teratogenic in the rat if given at doses 40the MRHD.

Breastfeeding

Trimethoprim enters human breast milk with an average level of 2-6mg/L and an M:P of 1.25. The theoretic infant dose can be calculated at 0.8mg/kg/d, which should not pose a risk. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. Bacteriuria, with or without clinical symptoms, is common during pregnancy. If left untreated, 20-30% of patients develop acute pyelonephritis, which increases the risk of preterm labor and low-birth-weight infants. Established first-line drugs such as amoxicillin, ampicillin, and trimethoprim-sulfamethoxazole are associated with a high degree of resistance in E. coli, the most common pathogen in the urinary tract. Nitrofurantoin or a b-lactam agent are also first-line agents for the treatment of asymptomatic bacteriuria. There are no adequate reports or well-controlled studies of trimethoprim-sulfamethoxazole in pregnant women (see the entries for the individual drugs). However, the most powerful study to date documents an increased prevalence of placenta-mediated adverse events when trimethoprim is given: preeclampsia, severe preeclampsia, placental abruption, IUGR, and fetal death. A growing number of women are being treated with trimethoprim in combination with an array of antivirals for HIV-related complications. The impacts of these combinations are poorly studied. Trimethoprim- sulfamethoxazole is also used for the treatment of Q fever during pregnancy. Women who develop Q fever should be treated for the duration of pregnancy, specifically if infected during the 1st trimester.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Transfer of trimethoprim across the human placenta is limited. While there is no solid evidence of teratogenicity in humans, the possibility it is a weak human teratogen cannot be excluded. In contrast, sulfamethoxazole readily crosses, reaching an F:M ratio approximating unity even in the 1st trimester. (See the entries for the individual drugs.) The combination has been associated with an increased risk of IUGR, CV, NTD, and urinary tract malformations.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Trimethoprim enters human breast milk, but the kinetics remain to be elucidated. It is unknown whether sulfamethoxazole enters human breast milk. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. Trimetrexate with leucovorin may have lower toxicity than trimethoprim-sulfamethoxazole. There is no published experience with trimetrexate during pregnancy. Recent concerns regarding the safety of trimethoprim suggest trimetrexate should be avoided during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether trimetrexate crosses the human placenta. Trimetrexate (without leucovorin) is teratogenic in rodents with increased risks of skeletal, visceral, ocular, and CV abnormalities.

Breastfeeding

There is no published experience in nursing women. It is unknown whether trimetrexate enters human breast milk. 1134 Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. Depression is common during and after pregnancy, but typically goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. There is no published experience with trimipramine during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether trimipramine crosses the human placenta. Rodent studies are generally reassuring, revealing no evidence of teratogenicity, though embryotoxicity was noted at the highest doses.

Breastfeeding

There is no published experience in nursing women. It is unknown whether trimipramine enters human breast milk. 1135

Pregnancy

. This 1st generation antihistamine is often paired illicitly with pentazocine to produce euphoria. Known as T?s and Blues, users have a greater risk of adverse

Pregnancy

outcome. There are no adequate reports or well-controlled studies of tripelennamine in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether tripelennamine crosses the human placenta. However, fetuses of women who abuse T?s and Blues have significantly reduced birth weight, length, and head circumference. Withdrawal occurs in about 1/3. Children of mothers who abused T?s and Blues throughout

Pregnancy

demonstrate interactive deficits and withdrawal similar to methadone-addicted newborns. The limited rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether tripelennamine enters human breast milk.

Pregnancy

. There is no published experience with trovafloxacin during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Trovafloxacin crosses the human placenta by simple diffusion and is unlikely to reach toxic levels. Rodent studies conducted with more than 10the MRHD reveal fetal toxicity and an increased prevalence of skeletal malformations.

Breastfeeding

There is no published experience in nursing women. The manufacturer reports that low levels of trovafloxacin are excreted into human breast milk, with levels ranging from 0.3 to 2.1mg/L after 200mg PO preceded by a load of 300mg IV. The theoretic infant dose of 120mcg/kg/d is unlikely to result in a clinically relevant level.

Pregnancy

. Tubocurarine is the active ingredient of the curare-producing plant Chondodendron tomentosum. Nondepolarizing relaxants are longer acting than depolarizing muscle relaxants. While there are no adequate reports or well-controlled studies of tubocurarine in pregnant women, there is a long clinical experience. Magnesium sulfate therapy prolongs the effect of tubocurarine. Long-acting agents such as tubocurarine or pancuronium have generally been abandoned by anesthesiologists/intensivists in favor of synthetic short- to intermediate-acting agents (e.g., cisatracurium, rocuronium, vecuronium) that have lesser side effect (e.g., histamine release, tachycardia) profiles.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Placental transfer of tubocurarine is greater than atracurium, with an F:M ratio of 0.09 for atracurium and 0.12 for tubocurarine (p < 0.05). However, it may be more rapidly cleared by the neonate. Tubocurarine is well-tolerated by the neonate if used during cesarean delivery, provided the interval between drug and delivery is short (1-10min). One woman treated for tetanus at 10-12w with tubocurarine for 10d delivered a term infant with joint contractures. Tubocurarine is administered directly to the fetus (3 or 1.5mg/kg SEFW IM/IV) to facilitate fetal therapeutic efforts. It lowers HR and BP in comparison to pancuronium. The duration of action of tubocurarine is directly related to the relative sensitivities of the different muscle groups, which are ranked from most sensitive to least sensitive as extraocular muscles, nuchal muscle, and diaphragm. Rodent studies reveal an increase in deformations consistent with absent fetal muscle tone.

Breastfeeding

There is no published experience in nursing women. It is unknown whether tubocurarine enters human breast milk. However, considering the indication and dosing, one-time tubocurarine use is unlikely to pose a clinically significant risk to the Breastfeeding neonate. 1139

Pregnancy

. There are no adequate reports or well-controlled studies of urea in pregnant women. Intra-amniotic urea is a valuable adjunct for late

Pregnancy

termination. There is no published experience in pregnant women for the remaining listed indications.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Urea crosses the human placenta. Intra-amniotic injection of urea (80-120g) in combination with a prostaglandin is used for 2nd and 3rd trimester termination. The urea is typically lethal when given prior to skin keratinization. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There is no published experience in nursing women. Urea likely enters human breast milk, but the effect of its use for the listed indications has not been studied. However, most of the urea ingested by the infant is not bioavailable. Thus any increase in milk urea from maternal treatment should be clinically irrelevant.

Pregnancy

. Urokinase is produced by the kidney and excreted in the urine. Urokinase treatment must be instituted as soon as possible after onset of PE, and no later than 7d. Therapy should be instituted within 6h of symptom onset if used to treat coronary artery thrombosis associated with an evolving transmural MI. Any delay instituting lytic therapy, even to evaluate the effect of heparin, decreases the potential for optimal efficacy. The diagnosis of a thromboembolus should always be confirmed by objective testing. Concurrent use of anticoagulants with IV administration of urokinase is not recommended except as noted. There are no adequate reports or well-controlled studies of urokinase in pregnant women. The published literature consists of case reports using urokinase to treat MI, PE, and cerebral and ovarian vein thrombosis either during

Pregnancy

or in the puerperium. Hemorrhage is common during pregnancy. In one series of 8 pregnant women with acute ischemic stroke treated, 2 suffered extracranial and 2 asymptomatic intracranial hemorrhages.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether urokinase crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether urokinase enters human breast milk. Plasminogen and plasminogen activator are normal components of breast milk. Considering the indications and dosing, one-time urokinase use is unlikely to pose a clinically significant risk to the Breastfeeding neonate. 1142

Pregnancy

. Ursodiol (ursodeoxycholic acid) is a naturally occurring human bile acid found in small quantities, but found in large quantities 1143 in the bile of certain bears. Small series suggest it can be effective for the treatment of cholestasis of

Pregnancy

(approximately 16mg/kg). Intrahepatic cholestasis of

Pregnancy

is a diagnosis of exclusion. It is associated with increased perinatal morbidity and mortality. Pruritus and postpartum hemorrhage are the main causes of maternal morbidity. Current management focuses on regular fetal and maternal monitoring and delivery at fetal maturity. However, a decrease in bile acids does not necessarily imply improved fetal outcome, and planned delivery remains prudent. One modest RCT concluded its combined use with S-adenosyl-L-methionine improved maternal responses. There is a case report of a woman with primary biliary cirrhosis treated throughout pregnancy. Ursodiol was effective, though a preterm cesarean delivery was required for uteroplacental dysfunction.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Ursodiol apparently does not cross the human placenta. It does, however, induce placental MRP2 expression, and reduce bilirubin and bile acid levels in umbilical cord blood.

Breastfeeding

Ursodiol does not enter human breast milk.

Pregnancy

. After ingestion, valacyclovir is metabolized to and actually enhances acyclovir bioavailability. It is effective and well tolerated for HSV suppression for up to 10y of continuous use. Neonatal herpes affects 1/15,000 newborns. The vast majority of infected infants are born to women with a primary infection during pregnancy. While there are no adequate reports or well-controlled studies of valacyclovir in pregnant women, it is used extensively for the listed indications. If initiated prophylactically at 36w, acyclovir reduces both the risk of recurrence and the frequency of a positive cervical culture at delivery in women who experience either a primary infection or at least one secondary episode during pregnancy. There is insufficient evidence to determine if antiviral prophylaxis reduces the incidence of neonatal herpes. However, patients should be counseled that antenatal antiviral prophylaxis reduces viral shedding and recurrences at delivery and reduces the need for cesarean delivery for genital herpes.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Valacyclovir crosses the human placenta. Maternal oral administration of valacyclovir leads to therapeutic concentrations in the maternal and fetal compartments, and in the instance of CMV, a decrease in the fetal viral load. However, it is unknown whether this decrease in CMV number is associated with decreased perinatal damage. Acyclovir crosses the rodent placenta. Post-marketing surveys suggest no increased frequency of birth defects. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Valacyclovir is converted to acyclovir, which enters human breast milk. However, the amount of acyclovir in breast milk during valacyclovir administration is <5% of the dose used to treat neonates.

Pregnancy

. Valdecoxib is an NSAID with anti-inflammatory, analgesic, and antipyretic properties. In general, the COX-2 inhibitors are associated with a lower incidence of GI upset but potentially an increase in MI. Valdecoxib provides effective relief of dysmenorrhea, but does not appear to be more effective than alternative, nonselective NSAIDs. The manufacturer removed the drug from the US market after 1146 concerns were raised about possible increased risks of MI and CVA. There is no published experience with valdecoxib during pregnancy. Its addition after cesarean delivery under spinal anesthesia with intrathecal morphine does not improve outcome. It has no effect on the timing of onset of rodent labor.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether valdecoxib crosses the human placenta. Other NSAIDs do cross and are associated with gastroschisis (1st trimester exposure), oligohydramnios, and ductal constriction. Valdecoxib increases the risk of skeletal malformations in some rodents when given at >70the MRHD. IUGR is noted with doses >5the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether valdecoxib enters human breast milk. It is found in rodent milk.

Pregnancy

. Valganciclovir is metabolized to ganciclovir. There is no published experience with valganciclovir during

Pregnancy

(see ganciclovir).

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Valganciclovir crosses the isolated human placenta by passive diffusion. Ganciclovir is embryotoxic and teratogenic in various rodent models. Birth defects include cleft palate, craniofacial abnormalities, and pancreas and renal agenesis.

Breastfeeding

There is no published experience in nursing women. It is unknown whether valganciclovir enters human breast milk. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission. (See Ganciclovir.)

Pregnancy

. Valproate is the sodium salt of valproic acid. There are no adequate reports or well-controlled studies of valproate in pregnant women. There is a long clinical experience with valproate. It does not alter the efficacy of hormonal contraception. Patients planning

Pregnancy

should be counseled on the risks and the importance of periconceptional folate supplementation.

Fetal Health

Valproate is a recognized human teratogen, increasing the relative risk by a factor of 4 with an overall prevalence of about 6%. The risk is compounded by a low serum folate. Valproate is rapidly and actively transported across the human placenta, reaching an F:M ratio exceeding 2. Recent

Pregnancy

databases suggest valproate is significantly more teratogenic than carbamazepine, and the combination of valproate and lamotrigine is particularly teratogenic. For unknown reasons, valproate accumulates in the fetal plasma. A distinct facial appearance, coupled with a cluster of minor and major anomalies and CNS dysfunction, characterize the fetal valproate syndrome. The likelihood of the offspring being affected is dose-dependent. Ten percent die in infancy, and 1/4 survivors have either developmental deficits or mental retardation. Affected fetuses may have an increased nuchal translucency measurement. A fetal medicine specialist should 1149 evaluate women taking valproate during pregnancy. As for most psychotropic drugs, monotherapy and the lowest effective quantity given in divided doses to minimize the peaks can theoretically minimize the risks. In one recent study, the outcomes of 154 valproate-exposed pregnancies (96% at least in the 1st trimester) were compared with those of 1315 unexposed pregnancies. The major anomaly rate in the valproate group exposed in the 1st trimester was higher than controls after exclusion of genetic or cytogenetic anomalies (6.7% vs. 2.5%, relative risk [RR] = 2.66). Five of the 8 major anomalies in the valproate group were CV, 2/8 were mental retardation, 2/5 male infants with major anomalies had hypospadias and 3/8 were suspected of having fetal valproate syndrome. A daily dose >1000mg was associated with the highest teratogenic risk (RR = 8.72). In the subgroup exposed to polytherapy, there was a 4-fold increase in the rate of major anomalies compared with controls. All major anomalies were in the group treated for epilepsy. In another study, those exposed to polytherapy in utero had significantly lower developmental quotients than those exposed to monotherapy. Polytherapy was a stronger predictor of lower developmental quotients than dose. Compared with carbamazepine monotherapy, valproate monotherapy was associated with significantly lower mental and motor developmental scores.

Breastfeeding

Valproate enters human breast milk, but the neonatal concentration is <10% of the maternal.

Pregnancy

. Most pregnancies are uneventful in women with epilepsy, and most babies are delivered healthy with no increased risk of obstetric complications in women. There is a long clinical experience with valproic acid. It does not alter the efficacy of hormonal contraception. Patients planning

Pregnancy

should be counseled on the risks and the importance of periconceptual folate supplementation.

Fetal Health

Valproate is a recognized human teratogen, increasing the relative risk by a factor of 4 with an overall prevalence of about 6%. The risk is compounded by a low serum folate. Valproate is rapidly and actively transported across the human placenta, reaching an F:M ratio exceeding 2. Recent

Pregnancy

databases suggest valproate is significantly more teratogenic than carbamazepine, and the combination of valproate and lamotrigine is particularly teratogenic. For unknown reasons, valproate accumulates in the fetal plasma. A distinct facial appearance, coupled with a cluster of minor and major anomalies and CNS dysfunction, characterize the fetal valproate syndrome. The likelihood of the offspring being affected is dose-dependent. Ten percent die in infancy, and 1/4 survivors have either developmental deficits or mental retardation. Affected fetuses may have an increased nuchal translucency measurement. A fetal medicine specialist should evaluate women taking valproate during pregnancy. As for most psychotropic drugs, monotherapy and the lowest effective quantity given in divided doses to minimize the peaks can 1152 theoretically minimize the risks. In one recent study, the outcomes of 154 valproate-exposed pregnancies (96% at least in the 1st trimester) were compared with those of 1315 unexposed pregnancies. The major anomaly rate in the valproate group exposed in the 1st trimester was higher than controls after exclusion of genetic or cytogenetic anomalies (6.7% vs. 2.5%, relative risk [RR] = 2.66). Five of the 8 major anomalies in the valproate group were CV, 2/8 were mental retardation, 2/5 male infants with major anomalies had hypospadias and 3/8 were suspected of having fetal valproate syndrome. A daily dose >1000mg was associated with the highest teratogenic risk (RR = 8.72). In the subgroup exposed to polytherapy, there was a 4-fold increase in the rate of major anomalies compared with controls. All major anomalies were in the group treated for epilepsy. In another study, those exposed to polytherapy in utero had significantly lower developmental quotients than those exposed to monotherapy. Polytherapy was a stronger predictor of lower developmental quotients than dose. Compared with carbamazepine monotherapy, valproate monotherapy was associated with significantly lower mental and motor developmental scores.

Breastfeeding

Valproic acid enters human breast milk, but the neonatal concentration is <10% of the maternal.

Pregnancy

. Valsartan has no significant advantages over similar agents in its class for which there is more experience. Nor has it been demonstrated to reduce the complications of arterial hypertension. There are no adequate reports or well-controlled studies of valsartan in pregnant women. Only a half dozen

Pregnancy

exposures are reported, some with poor outcomes typical of this drug class. Inhibitors of the renin-angiotensin system should be avoided during

Pregnancy

because of their fetal implications.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Drugs that act directly on the renin-angiotensin system can cause perinatal morbidity and death. Adverse outcomes are reported for valsartan suggesting it crosses the human placenta. Drugs that inhibit the fetal renin-angiotensin system are now recognized to be potentially teratogenic throughout gestation; the risks are greatest after the 1st trimester. The mechanisms may well be different for ACEIs and AT-1 receptor antagonists. In the 2nd and 3rd trimester, morbidity includes hypotension, neonatal skull hypoplasia, anuria, and reversible or irreversible renal failure. Oligohydramnios may be associated with limb contractures, craniofacial deformation, and hypoplastic lung development. Rarely, an alternative drug is not available. In these cases, the women should be counseled on the hazards, and serial ultrasound examinations should be performed to assess the intra-amniotic environment. If oligohydramnios is observed, the valsartan should be discontinued unless lifesaving for the mother. Antenatal surveillance may be appropriate depending upon gestation. Oligohydramnios may not appear until after the fetus has sustained irreversible injury.

Breastfeeding

There is no published experience in nursing women. It is unknown whether valsartan enters human breast milk.

Pregnancy

. Vancomycin is most commonly used for the treatment of MRSA infections. There are no adequate reports or well-controlled studies of vancomycin in pregnant women. In one series, adverse events were common, suggesting that longer infusion times and weight-adjusted doses should be used. It is used as a second-line agent for the treatment of postpartum endomyometritis, and as a first-line agent and alternative to metronidazole for the treatment of C. difficile diarrhea. Other applications during

Pregnancy

include listeriosis and bacterial endocarditis in IV drug users.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Vancomycin crosses the human placenta in a predictable manner, achieving concentrations that exceed the usual GBS inhibitory level. In contrast, transplacental passage of vancomycin was minimal in an ex vivo human placental perfusion model, yielding no detectable accumulation. There is no obvious explanation. Concern that vancomycin exposure might cause ototoxicity has not been substantiated. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Vancomycin enters human breast milk, but the kinetics remain to be elucidated. Considering the poor oral absorption, it is unlikely the breastfed neonate would ingest a clinically relevant amount.

Pregnancy

. Varicella is a cause of significant maternal and fetal morbidity and mortality. The attack rate of natural varicella after household exposure among healthy susceptible people approaches 90%. Varicella vaccine is a live, attenuated preparation, and as such is usually contraindicated during pregnancy. Most adverse events associated with varicella vaccine are minor, and serious complications rare. If vaccine virus transmission occurs, it does so at a very low rate and possibly without recognizable clinical disease. Most complications are instead associated with wild-type virus. Seventy percent of women in North America who do not remember having childhood varicella are actually immune. It is wise to test women of reproductive age planning pregnancy, and selectively immunize preconception if indicated. It is estimated that selective serologic screening of pregnant women with postpartum vaccination of susceptible women is cost-effective and would prevent half the cases of congenital varicella. There are no adequate reports or well-controlled studies of varicella vaccine in pregnant women. Inadvertent administration during

Pregnancy

produces maternal immunity. There are reports of its erroneous administration when varicella-zoster immune globulin was ordered.

Fetal Health

Varicella is a human teratogen. Abnormalities are usually related to CNS and peripheral nerve infection. They include skin lesions in dermatomal distribution, neurologic disease, and skeletal anomalies. The frequency of the syndrome is low (0.4-1.2% of infected cases) and gestational age related. There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether the attenuated virus comprising the varicella vaccine crosses the human placenta. Wild-type virus does cross. Inadvertent immunization during

Pregnancy

is unassociated with fetal pathology and is not a priori an indication for

Pregnancy

termination. A voluntary

Pregnancy

Registry established by the manufacturer (Merck & Co.) recorded 981 women inadvertently vaccinated during the 1st trimester between 1995 and 2005, among whom the

Pregnancy

outcomes were known. There was no evidence of congenital varicella syndrome and the major birth defect rate was 3.7%. Longitudinal study demonstrates the fetal immunologic response to congenital varicella may not be sustained. Molecular testing is recommended. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience with varicella vaccine in nursing women. According to one study by the manufacturer, it does not appear to enter human breast milk. Twelve women were enrolled postpartum; all seroconverted after the first vaccine dose. Varicella DNA was not detected by polymerase chain reaction 1158 (PCR) in any of the 217 postvaccination breast milk specimens. None of the infants was seropositive. Samples from 6 infants were tested for varicella-zoster virus DNA by PCR, and all were negative. In contrast, wild-type virus is excreted into human breast milk and can cause neonatal infection.

Pregnancy

. Varicella is a cause of significant maternal and fetal morbidity and mortality. Varicella pneumonia is perhaps the most serious maternal complication, with mortality rates in excess of 10%. Current smokers and women with more than 100 lesions are at particularly high risk. There are no adequate reports or 1159 well-controlled studies of varicella-zoster immune globulin in pregnant women. There is no evidence that administration to a susceptible, pregnant woman prevents viremia, fetal infection, or congenital varicella syndrome. The goal is to reduce the maternal sequelae of varicella rather than to prevent intrauterine infection. Women with no history of varicella and an unknown immune status should be tested as soon as the exposure is recognized. Seventy percent of women with no history of childhood varicella are immune. Varicella-zoster immune globulin administered within 24h of exposure may reduce the severity of maternal disease and is typically coupled with a course of acyclovir. The newer IV form achieves higher initial anti-varicella antibodies than the IM format. Though the effectiveness of this practice is unclear, case series indicate improved outcomes. Neonatal studies suggest the combination of immune globulin and acyclovir is more effective than monotherapy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is likely varicella-zoster immune globulin crosses the human placenta, but it is unknown whether such transfer conveys a level of passive immunity. Neonatal varicella is more likely severe when the maternal rash appears 5d prior to or 2d after delivery. These newborns should receive immune globulin immediately. Intravenous acyclovir is recommended for severely affected neonate. Unlike primary varicella infection in pregnancy, herpes zoster has not been documented to cause complications unless in the disseminated form. Newborns of women who develop varicella 7d before or up to 28d after delivery should be given varicella- zoster immune globulin and possibly acyclovir.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether varicella-zoster immune globulin enters human breast milk. Other IgG immunoglobulins do, and Breastfeeding is encouraged as a potential source of neonatal passive immunization.

Pregnancy

. V1 receptors are widely distributed in smooth muscle, including the myometrium. Women with dysmenorrhea have higher vasopressin levels. There are no adequate reports or well- controlled studies of vasopressin in pregnant women. Doses of vasopressin sufficient for an antidiuretic effect are unlikely to produce tonic uterine contractions deleterious to the fetus or threaten the continuation of the pregnancy. DDAVP is now the first choice for the treatment of diabetes insipidus and von Willebrand?s disease. It has also been used to treat gestational diabetes insipidus.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether vasopressin crosses the human placenta. Rodent teratogenicity studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Little vasopressin enters human breast milk, and it does not pose a significant risk to the Breastfeeding neonate.

Pregnancy

. Vecuronium is a nondepolarizing neuromuscular blocker. There are no adequate reports or well-controlled studies of vecuronium in pregnant women. Popular during cesarean delivery as an adjunct to general anesthesia, its effect may be prolonged by the concurrent administration of magnesium sulfate and possibly clindamycin.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. A limited amount of vecuronium crosses the human placenta within 5min, achieving a fetal concentration of 79ng/ml and an F:M ratio <0.07. It is administered directly to the fetus as an alternative to pancuronium during fetal procedures. In contrast to pancuronium, vecuronium has no effect on the FHR. This is an advantage for many procedures, but a potential drawback when used with fetal intravascular transfusion. Fetal paralysis modestly reduces oxygen consumption. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether vecuronium enters human breast milk. Though similar to pancuronium, vercuronium?s clearance is faster and t/2 shorter. Considering the indication and dosing, limited vecuronium use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Depression is common during and after pregnancy, but typically goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. There are no adequate reports or well-controlled studies of venlafaxine in pregnant women. In one woman, the elimination t/2 declined from 8.7h to 3.2h from the 1st to 3rd trimesters. Plasma levels likewise declined. Venlafaxine may be effective for the treatment of other disorders, including OCD, panic disorder, eating disorders, substance abuse, headaches, hot flashes, and chronic pain (including neuropathic pain).

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Venlafaxine and its active metabolites cross the human placenta and enter the AF, where it is actually concentrated. The M:F ratio approaches unity. Case-control study suggests it is unassociated with an increased prevalence of fetal malformations. Neonatal behavioral signs are noted in exposed more frequently than unexposed newborns, but symptoms are described as transient and self-limited. Premature infants could be more susceptible to the effects of SSRIs and venlafaxine. Rodent studies are generally reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. IUGR is seen in some models.

Breastfeeding

Venlafaxine enters human breast milk, achieving an M:P ratio approximating 2.5, and 2.7 for its active metabolite. Yet, the mean total drug exposure of breastfed infants is only 6.4%. Though this level of exposure should be safe, measurable levels are achieved in about1=2 of the exposed neonates, suggesting the need for close monitoring.

Pregnancy

. In addition to the listed indications, verapamil is used in some locales for the treatment of bipolar disorder and for tocolysis in women with preterm labor. There are no adequate reports or well- controlled studies of verapamil in pregnant women. There is no randomized or case-control study using verapamil as the primary tocolytic, and the practice of combining it with a b-blocker has been appropriately abandoned. Isolated case reports describe its successful use to treat maternal SVT. There are also rare reports of its use to treat preeclamptic hypertension, though there is no suggestion it offers advantages over other, more commonly used antihypertensives. Clearance is not altered in the rabbit pregnancy. Recently, a relationship between oral erythromycin and sudden cardiac death was reported in patients also receiving strong inhibitors of CYP3A (e.g., diltiazem, nitroimidazole antifungal agents, troleandomycin, verapamil); each doubles, at least, the AUC for a CYP3A substrate. Caution is advised.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Verapamil readily crosses the human placenta, achieving an F:M ratio of 0.7. Similar levels are found in AF. Relaxation of precontracted placental arteries by verapamil is reduced in placentas obtained from preeclamptic women. Doppler-determined fetal blood flow resistances in preeclamptic women are unaltered by verapamil. Verapamil has been used as transplacental therapy for fetal SVT with unclear efficacy. Flecainide remains the drug of choice for SVT and fetal hydrops. Direct fetal administration has been reported with success. Verapamil crosses the rabbit placenta, though the kinetics remain to be elucidated. Rodent studies are generally reassuring, revealing no teratogenicity despite the use of doses higher than those used clinically. However, IUGR and embryotoxicity occur.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Verapamil enters human breast milk, but the amount excreted is <0.05% and does not result in measurable levels in the nursing newborn.

Pregnancy

. Vidarabine is a purine nucleoside obtained from fermentation cultures of Streptomyces antibioticus. There is no published experience with vidarabine for the above indications during pregnancy. Treatment for encephalitis should be discontinued when the brain biopsy is negative for HSV in cell culture. Many of the previous uses for vidarabine have been superceded by acyclovir.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether vidarabine crosses the human placenta. Vidarabine is teratogenic in rodents after parenteral administration, where it appears to interfere with placental transport of uridine and adenosine. Though this concern remains for topical administration, it is unlikely the maternal systemic concentration will reach clinically relevant level. Vidarabine is used for neonatal treatment.

Breastfeeding

There is no published experience in nursing women. It is unknown whether vidarabine enters human breast milk. It is unlikely to pose a clinically significant risk to the Breastfeeding neonate after topical use.

Pregnancy

. Vinblastine is a vinca alkaloid. Fertility is retained when vinblastine is used for either GTD or ovarian cancer after ovary-sparing surgery. There are no adequate reports or well-controlled studies of vinblastine in pregnant women. The literature consists of numerous but isolated case reports of its use for the treatment of various malignancies.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether vinblastine crosses the human placenta. In vitro, its transfer involves P-glycoprotein, whose back-transfer of vinblastine may help protect the fetus. Most fetuses exposed deliver without apparent adverse effects. The risk of birth defects in pregnant women previously treated is similar to the background rate. Vinblastine is teratogenic and embryotoxic in rodents. Exposed fetuses should be evaluated in a fetal medicine unit.

Breastfeeding

There is no published experience in nursing women. It is unknown whether vinblastine enters human breast milk.

Pregnancy

. Vincristine is a vinca alkaloid. There are no adequate reports or well-controlled studies of vincristine in pregnant women. The literature consists of isolated case reports and series of women typically treated during

Pregnancy

for leukemia or lymphoma.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether vincristine crosses the human placenta. In vitro, its transfer involves P-glycoprotein, whose back-transfer may help protect the fetus. Most fetuses exposed deliver without apparent adverse effects. Vincristine is teratogenic and embryotoxic in rodents, and in limited study teratogenic in a subhuman primate. Exposed fetuses should be evaluated in a fetal medicine unit.

Breastfeeding

There is no published experience in nursing women. It is unknown whether vincristine enters human breast milk. It inhibits goat milk production in a dose-dependent manner.

Pregnancy

. Vinorelbine is a vinca alkaloid. There are no adequate reports or well-controlled studies of vinorelbine in pregnant women. The literature consists of multiple case reports of women treated during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether vinorelbine crosses the human placenta, though in vitro studies suggest a role for P-glycoprotein. The case reports of its use during

Pregnancy

usually note no adverse effects on the perinate attributable to treatment.

Breastfeeding

There is no published experience in nursing women. It is unknown whether vinorelbine enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of voriconazole in pregnant women. The published experience is limited to case reports of its use post?cesarean section for the treatment of Aspergillus.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether voriconazole crosses the human placenta.

Breastfeeding

There is no published experience in nursing women. It is unknown whether voriconazole enters human breast milk.

Pregnancy

. Thromboembolic disease remains a major cause of maternal morbidity and mortality. There are no adequate reports or well-controlled studies in pregnant women. It is most likely that a woman with a prior thromboembolic event unrelated to a permanent risk factor does not require prophylaxis during a subsequent pregnancy. The risk of a bleeding complication during

Pregnancy

approximates 18% with warfarin. An INR of 3.0 is sufficient for either prophylaxis or treatment of venous thromboembolism, thus minimizing the risk of hemorrhage associated with higher INRs. Women on warfarin planning

Pregnancy

should switch to a heparinoid agent prior to conception if possible. However, therapeutic heparin is not effective prophylaxis in women with a prosthetic heart valve, though some recommend replacement with heparin between 6 and 12w. A daily dose >5mg is associated with a greater risk of an adverse

Pregnancy

outcome. If the mother?s condition requires anticoagulation with warfarin, it should be substituted with heparin at 36w to decrease the risk to the fetus. Neuraxial anesthesia is contraindicated because of the risk of puncture- associated bleeding. Warfarin treatment is resumed postpartum. There is consensus those women with APL syndrome and their first DVT should be treated with warfarin to a target INR of 2.3-3.0. However, a recent systematic review including observational studies found patients with APL syndrome and stroke to be at a high risk of recurrent events. It may be reasonable to a target an INR>3.0 in this group. Likewise, the optimal approach for women with obstetric manifestations of APL syndrome is not well defined. Some recommend universal aspirin plus heparin, while others consider aspirin 1175 in monotherapy useful for women with recurrent early miscarriage only. Anticoagulation was evaluated in 60 pregnancies with a mechanical heart valve prosthesis and 45 with a tissue valve. All women had warfarin in the 2nd trimester and heparin for delivery. The 1st trimester was divided among warfarin only, heparin and LMWH. Live births occurred in 60% of tissue valves and 30% of mechanical valves. Likewise, spontaneous abortion rates differed with 2% in the tissue valves and 37% in the mechanical valves. The worst outcomes were with warfarin in the 1st trimester.

Fetal Health

Warfarin is a known teratogen. While there are no adequate reports or well-controlled studies in human fetuses, exposure from 6 to 10w gestation is associated with an embryopathy, and exposure subsequently with a fetopathy. The fetal warfarin syndrome includes nasal hypoplasia (failure of nasal septum development), microphthalmia, hypoplasia of the extremities, IUGR, heart disease, scoliosis, deafness, and mental retardation. While the embryopathy appears secondary to a fetal vitamin K deficiency, the fetopathy results from microhemorrhages. The most common CNS malformations include agenesis of the corpus callosum, Dandy-Walker malformation, and optic atrophy. In a large series of women treated the duration of

Pregnancy

for a prosthetic valve, the overall incidence of fetal warfarin syndrome was 5.6%. The

Pregnancy

loss rate was 32% and the stillbirth rate 10% of pregnancies achieving at least 20w. School-age children exposed in utero have an increased frequency of mild neurologic dysfunction and an IQ <80.

Breastfeeding

Warfarin does not enter human breast milk and is compatible with breastfeeding.

Pregnancy

. There is only limited published experience with zafirlukast during pregnancy. Leukotriene receptor antagonists are probably safe during

Pregnancy

but should be limited to special circumstances, where they are viewed essential for asthma control.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether zafirlukast crosses the human placenta. In one recent report, the subjects were participants of the Organization of Teratology Information Specialists Asthma Medications in

Pregnancy

Study. Perinatal outcomes among 96 women who took leukotriene receptor antagonists (LTRAs) (montelukast or zafirlukast) were compared with women who exclusively took short-acting b-agonists (n = 122) and women without asthma (n = 346). LTRAs use was not associated with an increased risk of

Pregnancy

loss, gestational diabetes, preeclampsia, low maternal weight gain, preterm delivery, low Apgar scores, or reduced measures of birth length and head circumference in infants. The prevalence of major structural defects in the LTRA group (5.95%) was higher compared with nonasthmatic controls (p = 0.007), but not different from the comparison group with asthma (p = 0.524). Furthermore, the defects observed in the LTRA group did not represent a consistent pattern. These findings suggests LTRAs are not a major human teratogen. Rodent and primate studies are reassuring, revealing no evidence of teratogenicity or IUGR (unless there was maternal toxicity) despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. Zafirlukast is excreted into human breast milk with an M:P ratio of 0.2.

Pregnancy

. There are no adequate reports or well-controlled studies of zalcitabine in pregnant women. The treatment of HIV during

Pregnancy

significantly reduces the risk of mother-to-child transmission. Triple therapy (lamivudine, nevirapine, zidovudine) remains the standard of care for management of HIV infection in adults. The FDA has approved only 4 nucleoside analog reverse transcriptase inhibitors: didanosine, stavudine, zalcitabine, and zidovudine. Zalcitabine is a 2nd selection should the patient not respond to zidovudine.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether zalcitabine crosses the human placenta. It does cross the primate (Macaca nemestrina) placenta. Rodent studies revealed evidence of teratogenicity at doses >1000the MRHD. 1180

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether zalcitabine enters human breast milk. However, Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. There is no published experience with zaleplon during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether zaleplon crosses the human placenta.

Breastfeeding

Small quantities of zaleplon are excreted into human breast milk. It is calculated that the Breastfeeding neonate would ingest approximately 0.015% of the maternal dose. This quantity is unlikely to result in a clinically relevant level.

Pregnancy

. There is no published experience with zanamivir during pregnancy. Pregnant women should consider vaccination prior to influenza season.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether zanamivir crosses the human placenta. It does cross the rodent placenta. Rodent studies are for the most part reassuring, with only minor skeletal abnormalities occurring in one strain of rat when the dose exceeded 1000the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether zanamivir enters human breast milk. It is excreted into rodent milk.

Pregnancy

. The treatment of HIV infection during

Pregnancy

significantly reduces the risk of mother-child transmission. Combination therapy (lamivudine, nevirapine, zidovudine) remains the standard of care for management of HIV infection in adults due to its high efficacy. The Pediatric AIDS Clinical Trials Group (protocol 076) documented that zidovudine chemoprophylaxis reduced perinatal HIV-1 transmission by nearly 70%. Since then, multiple randomized studies confirm zidovudine monotherapy is extremely effective in preventing vertical transmission of the virus. Shorter regimens reduced the risk of transmission by 50% in a non-

Breastfeeding

populations. When zidovudine is combined with other antiretroviral drugs (protease inhibitors), the effectiveness is almost 90%. The addition of nevirapine to the standard IV zidovudine labor regimen further reduces perinatal HIV transmission in women not already receiving antenatal antiretroviral therapy. The addition of nevirapine is not beneficial when the patient has been using ??triple therapy?? prenatally. It is possible in developed countries to lower the transmission rate below 4% using combinations of available medications and, for the selective patient, elective cesarean section before labor. Thus, it is important to encourage women to undergo testing for HIV during pregnancy, maximizing opportunities for offering antiretroviral therapy. Unfortunately, adherence to zidovudine therapy may be relatively low during the last 3w of gestation and during the first 3w postpartum. For women with HIV RNA levels of <1000copies/ml, a 3-part zidovudine prophylaxis regimen (prenatal, intrapartum, and neonatal) should be used alone or in combination with other antiretroviral drugs. Zidovudine prophylaxis is not associated with the development of resistance. Women should be monitored closely for hepatotoxicity after initiation of zidovudine. Side effects include agranulocytosis, thrombocytopenia, bone marrow suppression, seizures, anemia, pancreatitis, myopathy, lactic acidosis, granulocytopenia, hepatotoxicity, N/V, abdominal pain, diarrhea, headache, asthenia, rash, fever, anorexia, 1184 somnolence, myalgia, malaise, dyspepsia, diaphoresis, dyspnea, taste changes, pigmented nails, and paresthesias.

Fetal Health

Zidovudine and its major metabolites rapidly cross the human placenta, achieving concentrations that approach unity even in the 1st trimester. Maternal antiretroviral drug therapy during

Pregnancy

and labor, followed by 6w of neonatal zidovudine, significantly reduces the risk of vertical transmission. Additional antiretroviral drugs may be needed in some high-risk newborns. Asymptomatic women with HIV who lack a social support network are more likely not to comply with the recommended neonatal prophylactic regimen of antiretroviral therapy. Elective cesarean section prior to the onset of labor also reduces the rate of vertical transmission if there is a detectable maternal viral load. Mitochondrial disorders are described in children exposed to zidovudine in utero. MRIs observed in children with antiretroviral-induced mitochondrial dysfunction are similar to those in children with congenital mitochondrial diseases and even in exposed children without symptoms of systemic mitochondrial dysfunction. Fetuses exposed to triple therapy may be at increased risk for malformations.

Pregnancy

. There is no published experience with zileuton during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether zileuton crosses the human placenta. Rodent studies revealed evidence for an increased prevalence of IUGR, skeletal abnormalities, and cleft palate. 1186

Breastfeeding

There is no published experience in nursing women. It is unknown whether zileuton enters human breast milk. It is excreted into rodent milk.

Pregnancy

. There is no published experience with ziprasidone during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether ziprasidone crosses the human placenta. Rodent studies reveal evidence of embryotoxicity, IUGR, and an increased prevalence of malformation (cardiac, renal, and skeletal depending upon species and model) at doses similar to the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether ziprasidone enters human breast milk.

Pregnancy

.

Pregnancy

has a beneficial effect on migraine in 55-90% of women, mainly during the 2nd and 3rd trimesters. A higher percentage of women with menstrual migraine compared to other migraines improve during pregnancy. There is no published experience with zolmitriptan during pregnancy. Mean plasma concentrations of zolmitriptan are up to 1.5-fold higher in females than males. It is not known whether

Pregnancy

alters clearance.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether zolmitriptan crosses the human placenta. Rodent studies revealed embryotoxicity and skeletal abnormalities at doses more than 500the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether zolmitriptan enters human breast milk. It is excreted into rodent milk. However, considering the indication and dosing, one-time or occasional zolmitriptan use is unlikely to pose a clinically significant risk to the Breastfeeding neonate. If desired, the patient may pump her breasts for 24h and then resume breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of zolpidem in pregnant women. Zolpidem significantly inhibits smooth muscle contractility in vitro.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Zolpidem crosses the human placenta, but the kinetics have yet to be elucidated. Typical maternal peak levels after 5 or 10mg are 59 and 121ng/ml respectively. In one case report, the cord blood level at least 14h after maternal ingestion was 41ng/ml. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Prenatal exposure to diazepam and alprazolam, but not to zolpidem, affects behavioral stress reactivity in adult male rats.

Breastfeeding

Less than 0.02% of the total administered maternal dose is excreted into milk, but the effect of zolpidem on the infant is unknown. It seems unlikely the occasional use of zolpidem would pose a clinically insignificant risk to the Breastfeeding neonate. If desired, the patient may pump her breasts for 8h and then resume breastfeeding.

Pregnancy

. There are no interactions between zonisamide and the combined OCP, progesterone-only pill, medroxyprogesterone injections, or levonorgestrel implants. There are no adequate reports or well-controlled studies of zonisamide in pregnant women. Levels may decline with advancing gestation.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Zonisamide crosses the human placenta, achieving F:M ratios of 0.92. The current data do not indicate an increased risk of teratogenicity in humans. However, studies in rodents, dogs, and nonhuman primates reveal embryotoxicity and an increased prevalence of malformations when zonisamide is given at doses within the human range during organogenesis.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Zonisamide enters human milk, achieving an M:P ratio between 0.6 and 1.03. Using the available data, the theoretic infant dose would approximate 1.4mg/kg/d.

Pregnancy

. Migraine headaches are a frequent complaint during pregnancy, and ergot compounds are generally considered contraindicated. From 55% to 90% of pregnant women experience an improvement in headache symptoms during the 2nd and 3rd trimesters. A higher percentage of women with menstrual migraine find they improve during pregnancy. There are no adequate reports or well-controlled studies of naratriptan in pregnant women. The clearance of naratriptan is modestly reduced (22%) in women on oral contraceptives; clearance during

Pregnancy

is unstudied. Smoking increases clearance by 1/3. The manufacturer, Glaxo-Wellcome, maintains a registry for post-marketing information on

Pregnancy

outcomes.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Epidemiologic information is limited but reassuring. However, ther is more experience with sumatriptan. It is unknown whether naratriptan crosses the human placenta. Rodent studies reveal embryotoxicity and skeletal abnormalities at doses producing maternal plasma levels only a few multiples of the MRHD. However, the frequencies of these adverse outcomes are not dose-dependent. 761

Breastfeeding

There is no published experience in nursing women. It is unknown whether naratriptan enters human breast milk. It does enter rodent milk. However, considering the indication and dosing, one-time naratriptan use is unlikely to pose a clinically significant risk to the Breastfeeding neonate. The patient may choose to pump her breasts for 24h for added safety.

Pregnancy

. Oral agents have rapidly become established viable alternatives during

Pregnancy

in women with type 2 diabetes mellitus. Nateglinide is a D-phenylalanine derivative that helps reduce postprandial hyperglycemia. There is no published experience during pregnancy.

Fetal Health

There is no published experience in human fetuses. It is unknown whether nateglinide crosses the human placenta. Rodent studies are generally reassuring, though some note an increase in gallbladder agenesis at doses 40the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether nateglinide enters human breast milk. It is excreted into rodent milk, and the maternal administration of high doses slows pup weight gain. It is unknown whether the reduced growth reflects only maternal hypoglycemia.

Pregnancy

. There is no published experience with nedocromil during pregnancy. Nedocromil is effective long-term maintenance therapy for bronchial asthma.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether nedocromil crosses the human placenta. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level. Rodent studies are reassuring, revealing no evidence of 763 teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether nedocromil enters human breast milk. However, considering the indication and dosing, occasional nedocromil use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Depression is common during and after pregnancy, but typically goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. The serotonin reuptake inhibitors are first-line treatment for most depressive and anxiety disorders. Nefazodone is unrelated to SSRIs, TCAs, or MAOIs. There is limited published experience with nefazodone during pregnancy. It has been used to treat postpartum depression.

Fetal Health

There is no published experience in human fetuses. It is unknown whether nefazodone crosses the human placenta. A prospective case-control study was reassuring, revealing no evidence of an adverse fetal effect. Rodent studies are generally reassuring, revealing no signs of teratogenicity or IUGR despite the use of doses higher than those used clinically. There is an unexplained increase in early pup death. 764

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Nefazodone enters human breast milk, and neonatal drowsiness, lethargy, and poor feeding that resolves when Breastfeeding stops are reported. If the mother elects to breastfeed, the infant should be monitored for possible adverse effects, the drug given at the lowest effective dose, and

Pregnancy

. The incidence of both the AIDS syndrome and opportunistic infections has declined over the last few years due to advances in drug regimens. HAART consisting of 3-5 agents is the current standard of care in the US for the management of HIV infection during

Pregnancy

because of its high efficacy. Some study protocols use nelfinavir as the protease inhibitor. The treatment of HIV during

Pregnancy

dramatically reduces the risk of mother-to-child transmission in proportion to the maternal viral load.

Pregnancy

increases clearance. In one steady-state study of 20 women on a HAART regimen including nelfinavir (1250mg bid) and two NRTIs, during the 3rd trimester median nelfinavir AUC (0-12 h) was 25.8mcg/h/ml vs. 32.5mcg/h/ml in the control group. Median oral clearance (CL/F) was significantly higher in pregnant women (48.5 L/h vs. 38.5 L/h), but the difference disappeared when CL/F was adjusted for body weight. Trough concentration was also significantly (p <.01) lower during 766

Pregnancy

(median 0.8mcg/ml vs. 1.5mcg/ml). The elimination t/2 of nelfinavir during

Pregnancy

was 3.7h (range 1.4-6.6h), compared with 5.2h (range 3.1-10.1h) in the control group. A smaller study led to a similar conclusion. These results indicate that women in the later stages of

Pregnancy

may be exposed to subtherapeutic concentrations of nelfinavir if the dosage or frequency is not adjusted. This increased clearance takes some time to return to the prepregnant values. In one study of 9 pregnant women, clearance was unaltered compared to the puerperium. Careful monitoring for hepatotoxicity during therapy with nelfinavir is recommended. The association between combination antiviral therapy with protease inhibitors and an increased risk of very low birth weight requires confirmation. Nelfinavir-related GI symptoms and hyperglycemia may be more common during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Like most protease inhibitors, nelfinavir crosses the human placenta but achieves only subtherapeutic levels. In one study, the nelfinavir F:M concentration ratio was 25% for maternal concentrations of 0.1-2.5mg/L between 31 and 41w gestation. In another study, cord blood concentrations were below the limit of assay detection in 10 of 40 samples for nelfinavir and 10 of 16 AF samples. The transfer is probably limited by a high degree of plasma protein binding and backward transport by placental P-glycoprotein. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Nelfinavir enters human breast milk, but the M:P ratio ranges from 6% to 24%. Breastfeeding is contraindicated in HIV- infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. There are no adequate reports or well-controlled studies of neomycin in pregnant women. Neomycin is poorly absorbed in the bowel, though repeated dosing can lead to accumulation especially in the inner ear. Clearance can take weeks. The CDC recommends the use of a selective broth culture to improve detection of genital tract or anorectal carriage of GBS in pregnant women. The addition of neomycin to nalidixic acid in a selective broth medium improves the sensitivity of screening cultures for the detection of GBS carriage in women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether neomycin crosses the human placenta. While there is no evidence that it is a human teratogen, some aminoglycosides (e.g., streptomycin) have been associated with irreversible deafness after in utero exposure. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level after topical administration. Rodent teratogenicity studies have not been performed. Neomycin is used for prophylaxis of ophthalmia neonatorum, though efficacy has not been tested through clinical trials.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether neomycin enters human breast milk. Neomycin is excreted into both ovine and rat breast milk. However, considering the indication and dosing, occasional topical use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. There are case reports of use of neostigmine throughout

Pregnancy

for the treatment of maternal myasthenia gravis. It is also increasingly used for neuraxial anesthesia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether neostigmine crosses the human placenta. Twenty to 30% of offspring of women suffering from myasthenia gravis have transient neonatal motor symptoms, suggesting maternal antibodies cross the placenta. Newborns with myasthenia gravis require neostigmine until complete recovery of the motor handicap. Rodent teratogenicity studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether neostigmine enters human breast milk. However, considering the indications and dosing, occasional use is unlikely to pose a clinically significant risk to the Breastfeeding neonate. It is generally considered compatible with breastfeeding.

Pregnancy

. Nesiritide is human recombinant BNP. There is no published experience with nesiritide during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether nesiritide crosses the human placenta. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether nesiritide enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of netilmicin in pregnant women. It is the 1st alternative to gentamicin for the treatment of brucellosis. There are case reports of its use for listeriosis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether netilmicin crosses the human placenta. While there is no evidence that netilmicin is a human teratogen, some aminoglycosides (e.g., streptomycin) have been associated with irreversible deafness after in utero exposure. Rodent teratogenicity studies have not been performed. Transfer across the term rat placenta appears low. In the guinea pig, netilmicin had significantly less effect on the cochlea compared to gentamicin. In the rat, the impact of netilmicin on renal function after in utero exposure is similar to gentamicin and greater than amikacin.

Breastfeeding

There is no published experience in nursing women. A small amount of netilmicin enters human breast milk, but the kinetics remain to be elucidated.

Pregnancy

. The incidence of both the AIDS syndrome and opportunistic infection has decreased dramatically over the last years because of advances in drug regimens. This is a rapidly changing area. Triple (e.g., zidovudine, lamivudine, nevirapine) or quadruple therapy remains the standard of care for the management of HIV infection in adults because of its high efficacy. Nevirapine-based HAART (compared mainly with nelfinavir-based HAART), western African origin, and lower baseline viral load are associated with shorter times to achieving viral suppression and is probably a regimen of choice. A single dose of nevirapine (200mg PO) given at the onset of labor dramatically reduces perinatal HIV transmission in women receiving no other antenatal antiretroviral therapy. It is more effective (in the absence of regular antiretroviral therapy) than an intrapartum and postpartum regimen of zidovudine if given to both women at the onset of labor and their newborns within 72h of birth. Nevirapine resistance does occur from this approach. However, a single dose of tenofovir and emtricitabine at delivery reduces resistance to NNRTIs at 6w postpartum by half; therefore, this treatment should be considered as an adjuvant to intrapartum nevirapine. Women who receive a single dose of nevirapine to prevent perinatal transmission of HIV-1 have higher rates of failure with subsequent nevirapine-based antiretroviral therapy than do women without previous exposure to nevirapine if the therapy is initiated within 6mo after the single peripartum dose. Maternal risk factors include a low CD4cell count and a high viral load at delivery. The addition of nevirapine during the labor of women receiving antiretroviral therapy during

Pregnancy

does not further reduce perinatal HIV transmission if cesarean section is available. Cost and identification of women with HIV infection during

Pregnancy

represent a significant problem in many developing countries. As a result, it has been proposed that, in high HIV prevalence areas, ??triple therapy?? be offered routinely to all pregnant women and their infants without prior HIV testing. The association between combination therapy that includes a protease inhibitor and an increased risk of very low birth weight requires confirmation. Hepatotoxicity usually does not manifest before 5mo of therapy. The WHO takes an incremental approach, recommending countries adopt more effective antiretroviral regimens. The 2006 guidelines include triple-drug antiretroviral treatment for those women who are eligible. Those women who are not eligible for antiretroviral treatment should receive a combination prophylaxis antiretroviral regimen?preferably zidovudine from 28w of gestation; zidovudine, lamivudine, and a single dose of nevirapine during delivery; and zidovudine and lamivudine for 7d after delivery?to reduce the development of nevirapine resistance. Newborn infants should receive a single dose of nevirapine and 1-4w of zidovudine, depending on the duration of the regimen received by the mother.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. The safety of many approved antiretroviral agents during

Pregnancy

is not established. In contrast to other protease inhibitors, nevirapine rapidly crosses the human placenta, reaching an F:M ratio approximating unity. A single 2mg/kg dose administered to the newborn at 48-72h after birth achieves serum nevirapine concentrations 10the in vitro 50% inhibitory 774 concentration against wild-type HIV-1 throughout the 1st week of life. This limited regimen is well-tolerated and reduces the risk of mother-to-child transmission by nearly 50% in women and infants receiving no other antiretrovirals. However, neonatal plasma concentrations decrease more rapidly after maternal nevirapine therapy during pregnancy, suggesting in utero liver enzyme induction. Infants born <2h after maternal nevirapine during labor should receive a dose immediately after birth in addition to the standard infant dose at 48-72h to ensure therapeutic levels.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Nevirapine is excreted into human breast milk with an M:P ratio approximating 0.6. Breastfeeding is contraindicated in HIV-infected nursing women when formula is available to reduce the risk of neonatal transmission. However,

Pregnancy

. Niacin is a water-soluble B-complex vitamin with essential roles in lipid metabolism, tissue respiration, and glycogenolysis. The higher death rate from pellagra in women compared to men is attributed to an estrogen-mediated decrease in the formation of niacin from tryptophan.

Pregnancy

imposes a metabolic stress, which grows with advancing gestation. The recommended dose of niacinamide (a by-product of niacin) varies between 15 and 17mg/d, and it is usually found in prenatal vitamins. There are no adequate reports or well-controlled studies of niacin in pregnant women. Despite routine vitamin supplementation, a high percentage of vitamin A, B6, B12, niacin, and thiamine hypovitaminemia occurs during pregnancy. Niacin deficiency is particularly common during the 1st trimester and its prevalence increases subsequently. Combination deficits of niacin, thiamine, and vitamins A, B6, and B12occur in each trimester. There is no evidence that supplementation changes

Pregnancy

outcome. Niacin deficiencies were once thought associated with preeclampsia and hyperemesis gravidarium, but these associations were not confirmed by well-designed studies.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Niacin crosses the human placenta, though the 777 kinetics remain to be elucidated. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Niacin is excreted into human breast milk. It is not known whether supplementation increases both the milk and neonatal concentration. Niacin is generally considered compatible with breastfeeding.

Pregnancy

. Hypertension during pregnancy: Hypertension remains a significant cause of maternal and fetal morbidity and death. Severe hypertension during

Pregnancy

(BP >170/110mmHg) should be treated immediately to improve both maternal and fetal outcome. An uncontrolled reduction in BP may lead to coma, stroke, MI, acute renal failure, and death.

Pregnancy

further complicates the treatment of an acute hypertensive episode because an acute decrease in BP might adversely affect the fetus. Thus, the goal is not just to decrease BP, but to do so with minimal adverse effects while preserving organ function. Randomized trials reveal that nicardipine is safe and effective for the treatment of severe hypertension during pregnancy. It is more efficient than metoprolol and similar to labetalol. Although the definitive treatment for severe preeclampsia remains delivery, some practitioners attempt to temporize in hopes of reducing the complications of prematurity. Preliminary study indicates that long-term treatment with nicardipine for severe preeclampsia is effective and safe. Nicardipine has also been used during

Pregnancy

to treat hypertension due to pheochromocytoma and autonomic hyperreflexia. Preterm labor: Nicardipine abolishes in vitro contractility of the smooth muscle strips. It causes a modest decline in systolic (9mmHg) and diastolic (7mmHg) pressures in normotensive patients as peripheral resistance falls. The reflex increase in HR is usually small, but may occasionally be pronounced. One prospective clinical trial concluded that nicardipine is an effective, safe, and well-tolerated tocolytic agent. It arrests preterm labor more rapidly than magnesium sulfate, and women treated with nicardipine have fewer adverse medication effects and episodes of recurrent preterm labor compared to those treated with magnesium sulfate. Treatment-related maternal hypotension was not associated with fetal distress. In another trial, nicardipine led to a greater percentage of women delivering more than 7d after diagnosis compared to salbutamol, and there were fewer maternal Side effects include edema, flushing, asthenia, malaise, N/V, dyspnea, palpitations, tachycardia, dizziness, dry mouth, constipation, nervousness, nocturia, ECG abnormalities, and orthostatic hypotension.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. In one study of 10 preeclamptic women, nicardipine was measured in maternal and umbilical cord blood. There was a median F:M ratio of 0.15 (umbilical artery) and 0.17 (umbilical vein). The highest cord concentration after maternal dosage of 4.5mg/h was a subtherapeutic 18ng/ml. Thus, adverse fetal reactions are unlikely due to a direct nicardipine effect. Consistent with these observations, transfer across the nonhuman primate placenta is poor, and there is no effect on fetal CV parameters after maternal administration. Nicardipine may have 779 some beneficial effect on fetoplacental blood flow resistances in animals and humans. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity occurred at doses 50the MRHD. Breastfeeding Nicardipine levels were determined in 34 breast milk samples from 7 preeclamptic women receiving IV nicardipine. Nicardipine was undetectable in 82% of samples. In 6 samples from 4 women with doses ranging from 1 to 6.5mg/h, milk nicardipine ranged from 5.1 to 18.5ng/ml. The maximum possible exposure of a neonate to nicardipine was calculated to be less than 300ng/d, which is an insignificant fraction of the therapeutic dose used in neonates.

Pregnancy

. Cigarette smoking is directly linked to an array of health care problems whose costs to society are staggering. Active and passive maternal smoking has damaging effects in each trimester. Cigarette smoke contains numerous toxins that exert a direct effect on placental and fetal cell proliferation and differentiation. It is the single largest modifiable risk for pregnancy-related morbidity and death in the US. Cigarette smoking increases the rate of subfertility and failed IVF. Addiction to nicotine is a primary contributor to tobacco use. Nicotine replacement facilitates cessation by relieving the physiologic symptoms of withdrawal. Nicotine delivery systems include gum, patch, nasal spray, and vapor inhaler. Because nicotine medications do not deliver the toxins and carcinogens delivered by cigarettes, they are considered safer than smoking if used as directed. Women should be advised to stop smoking completely during pregnancy, and that 781 a simple reduction in the number of cigarettes smoked, or switching to so-called low-tar or low-nicotine concentration cigarettes will not significantly reduce the perinatal risks. Nicotine patch therapy may help some pregnant smokers, but the success rate during

Pregnancy

is low. Despite the failure of large numbers of treated women to quit, the average birth weight is increased by therapy. The success rate may be enhanced by the addition of an SSRI and formal counseling. Preliminary study suggests women who cannot quit smoking after the 1st trimester metabolize nicotine more rapidly than those who can. Thus, the optimal response may be to raise the support level during pregnancy, not lower it. Social support systems can enhance the likelihood of long-term success in women who do quit smoking during pregnancy. The initial dose of nicotine during replacement therapy should approximate the dose of nicotine being consumed. Intermittent-use formulations of NRT (gum, spray, inhaler) are preferred as the total dose of nicotine delivered to the fetus is less than with continuous-use formulations (transdermal patch).

Fetal Health

Cigarette smoke contains thousands of chemicals, many of which are well-documented reproductive toxins (e.g., nicotine, carbon monoxide, lead). Nicotine rapidly crosses the placenta, and the fetuses of mothers who smoke are exposed to higher concentrations than their mothers. Smoking during

Pregnancy

is a major risk factor for spontaneous abortion, preterm placental abruption, IUGR, late fetal death, neonatal polycythemia, and SIDS. The increased miscarriage rate among mothers who smoke may be related to direct adverse effects of nicotine, cadmium, or the polyaromatic hydrocarbons on trophoblast invasion and proliferation. The mean reduction in birth weight in infants of smokers is 200g. Recent study indicates a greater prevalence of facial clefts in the offspring of smokers. Longitudinal studies in humans suggest that prenatal exposure to nicotine increases the risks for cognitive deficits, ADHD, conduct disorder, criminality in adulthood, and a predisposition of the offspring to abuse tobacco and alcohol. Sheep and human studies reveal that prenatal nicotine blunts elements of the fetal cardiorespiratory defense for hypoxia (HR, ventilatory and arousal responses), and has long-term effects on the postnatal breathing pattern. The newborn unable to maximize cardiac output during times of stress is at increased risk for morbidity and possible death. Acute exposure to nicotine significantly decreases fetal heart reactivity. Median epinephrine and NE concentrations in the umbilical cord are significantly lower in smokers compared with nonsmokers. The significance of this finding is unclear, but could reflect depletion. The finding of increased connective tissue expression in pulmonary vessels of fetal monkeys whose mothers were treated with nicotine suggests nicotine is transported across the placenta and directly interacts with nicotinic ACH receptors in pulmonary vessels to alter connective tissue expression and produce vascular structural alterations. Rodent studies show that nicotine exposure compromises neuronal maturation, leading to long-lasting structural alterations in key brain regions involved with cognition, learning, and memory. Human neonatal nicotine withdrawal does occur.

Breastfeeding

Nicotine is excreted in human milk at low concentrations. Milk cotinine (a by-product of nicotine) levels do not correlate with 782 the number of cigarettes smoked. Newborns breastfed by smoking women are exposed not only to environmental (??passive??) smoke, but also by ingesting nicotine metabolites and toxic by- products present in the milk. Maternal smoking cessation with the nicotine patch is a safer option than continued smoking. In one study of 15 women, the milk nicotine and cotinine concentrations were no different between smoking (mean of 17 cigarettes/d) and the 21mg/d patch, but concentrations were lower when patients were using the 14mg/d and 7mg/d patches. There was also a downward trend in absolute infant dose (nicotine equivalents) from smoking or the 21mg patch through

Pregnancy

. Hypertension during pregnancy: Hypertension remains a significant cause of maternal and fetal morbidity and death. Severe hypertension during

Pregnancy

(BP >170/110mmHg) should be treated immediately to improve both maternal and fetal outcome. An uncontrolled reduction in BP may lead to coma, stroke, MI, acute renal failure, and death. Treatment of an acute hypertensive episode during

Pregnancy

further complicates the process because an acute decrease in BP might adversely affect the fetus. Thus, the goal is not just to decrease BP, but to do so with minimal adverse effects while preserving organ function. Nifedipine is proven safe and effective. The antihypertensive effect of nifedipine does not correlate with the serum concentration. Given PO or SL, nifedipine (8-10mg ?1) has a longer duration of action and is more effective than either IV hydralazine (5- 10mg ?1) or IV labetolol (20mg ?1). In randomized trials, nifedipine retard was as effective as the rapidly acting formuation, though women given the retard form required a 2nd dose more frequently. One approach is to observe the patient 24h to learn the proper timing of nifedipine. This is based on the observation that hypertension is more pronounced at night in women with preeclampsia compared to chronic hypertension. Maternal cerebral blood flow is influenced by antihypertensive treatment. A reduction in middle cerebral artery flow velocities after nifedipine and methyldopa confirms that cerebral vasospasm occurs in preeclamptic women. In contrast to the middle cerebral artery, there is no change in uteroplacental Doppler-determined resistances in severe preeclamptic women treated with nifedipine. Preterm labor: No tocolytic agent actually stops preterm labor or alone improves perinatal outcome. Tocolysis changes perinatal outcome by allowing time for corticosteroid administration. When compared to placebo and any other tocolytic agent, calcium channel blockers and specifically nifedipine reduce the number of women giving birth within 48h or 7d of diagnosis. The doses used ranged widely from 30 to 240mg/d until contractions stop; 40mg PO q4-6h seem the typical starting dose. Like all other tocolytic agents, maintenance use offers no added benefit. The frequency of drug discontinuation for adverse effects is also dramatically reduced for nifedipine compared to all other tocolytic agents. In steady state, the mean nifedipine plasma concentration to achieve tocolysis is about the half of that measured after initial tocolysis. The use of nifedipine with magnesium sulfate is potentially dangerous; the combination is more frequently associated with severe hypotension, neuromuscular blockade, and cardiac depression. Similar to all other agents, maintenance therapy with oral nifedipine after the successful treatment of presumed preterm labor does not alter the timing of delivery. Several case reports note the occurrence of acute MI during the use of nifedipine for tocolysis. A short interval between cessation of b-mimetic therapy and the start of nifedipine may have had a role. Recently, a relationship 785 between oral erythromycin and sudden cardiac death was reported in patients also receiving strong inhibitors of CYP3A such as nitroimidazole antifungal agents, diltiazem, verapamil, and troleandomycin; each doubles, at least, the AUC for a CYP

Breastfeeding

Nifedipine is excreted into human breast milk, achieving an M:P ratio approximating 0.3. It is unlikely the nursing newborn would ingest a clinically relevant amount.

Pregnancy

. Nimodipine is a calcium channel blocker with selective cerebrovascular effect. Hypertension during pregnancy: Hypertension remains a significant cause of maternal and fetal morbidity and death. Severe hypertension during

Pregnancy

(BP >170/110mmHg) should be treated immediately to improve both maternal and fetal outcome. An uncontrolled reduction in BP may lead to coma, stroke, MI, acute renal failure, and death.

Pregnancy

further complicates the treatment of an acute hypertensive episode since an acute decrease in BP might adversely affect the fetus. Thus, the goal is not just to decrease BP, but to do so with minimal adverse effects while preserving organ function. Cerebral perfusion pressure may be either high or low in women with preeclampsia and eclampsia. A recent Cochrane review concluded based on a series of adverse outcomes that nimodipine should be avoided for this indication. Specifically, it was associated with a higher risk of eclampsia (relative risk [RR] 2.24, 95% CI 1.06-4.73) and respiratory difficulties (RR 0.28, 95% CI 0.08-0.99). Nimodipine significantly reduces Doppler-measured resistances of the retinal vessels. 788 Compared to magnesium sulfate, nimodipine increases cerebral perfusion pressure in women with severe preeclampsia. While once suggested as an agent to prevent eclampsia, it is inferior to magnesium sulfate as prophylaxis. Preterm labor: When compared with any other tocolytic agent, calcium channel blockers reduce the number of women giving birth within 48h or 7d of diagnosis. The frequency of drug discontinuation for adverse effects is also dramatically reduced. There are no adequate reports or well-controlled studies of nimodipine for tocolysis in pregnant women. It is an effective inhibitor of uterine contractions in vitro. Either nifedipine or nicardipine would be preferable. Psychiatric disorders: Nimodipine may be an alternative to lithium in pregnant women with bipolar disorder.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Nimodipine crosses the human placenta, reaching an F:M ratio approaching unity within several hours. Maternal administration reduces both maternal and fetal cerebral resistances. Rodent studies are somewhat conflicting. Placental transfer is inefficient. Embryotoxicity, teratogenicity, and IUGR are reported in some models, but it occurs in a non?dose- dependent fashion.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Nimodipine enters human breast milk. In one case report, the M:P ratio approximated 0.1. It was estimated the breastfed newborn would ingest a clinically insignificant amount ranging between 0.008% and 0.092% of the weight-adjusted maternal dose.

Pregnancy

. Hypertension remains a significant cause of maternal and fetal morbidity and death. Severe hypertension during

Pregnancy

(BP >170/110mmHg) should be treated immediately to improve both maternal and fetal outcome. An uncontrolled reduction in BP may lead to coma, stroke, MI, acute renal failure, and death. Treatment of an acute hypertensive episode during

Pregnancy

further complicates the process, because an acute decrease in BP might adversely affect the fetus. Thus, the goal is not just to decrease BP, but to do so with minimal adverse effects while preserving organ function. In one study, nisoldipine was used to treat preeclamptic women with severe postpartum hypertension. A rapid and significant fall in BP was seen within 30min, and maintained successfully by repeating nisoldipine for the duration of the study period. There were no adverse reactions.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether nisoldipine crosses the human placenta. Nisoldipine was unassociated with changes in the FHR despite maternal bradycardia. Rodent studies conducted at doses that cause maternal toxicity were associated with embryotoxicity. 790

Breastfeeding

There is no published experience in nursing women. It is unknown whether nisoldipine enters human breast milk.

Pregnancy

. UTI is common during pregnancy, and all pregnant women should be screened. Treatment of asymptomatic bacteriuria and recurrent cystitis during

Pregnancy

reduces the risk of pyelonephritis. Ampicillin should not be used because of the high prevalence of resistant E. coli. Nitrofurantoin is highly soluble in urine. It is safe and effective for the treatment of asymptomatic bacteriuria as well as acute and recurrent UTIs. Resistance rates are <10%. Pyelonephritis occurs in approximately 7% of women despite adequate treatment. Women with recurrent UTI are 791 candidates for long-term antibiotic prophylaxis. Neither gravidity nor pyelonephritis alters the renal excretion or blood concentration of nitrofurantoin. However, labor reduces renal excretion and increases the blood level. Thus, nitrofurantoin is a poor selection for therapy during labor. Acute pulmonary reactions to nitrofurantoin, presumably immune-mediated, are uncommon but may be life-threatening. Symptoms include fever, chills, cough, pleuritic chest pain, dyspnea, pleural effusion, and pulmonary hemorrhage. The drug should be discontinued and corticosteroids initiated for severe reactions. Irreversible pulmonary fibrosis is also reported. Patients with G6PD deficiency may experience hemolytic reactions. It remains unclear how long a woman with asymptomatic bacteriuria should be treated, and there are no randomized studies. Some suggest that short-term administration combined with continued surveillance for recurrent bacteriuria is sufficient.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether nitrofurantoin crosses the human placenta. There is no evidence nitrofurantoin is a human teratogen. Although contraindicated in labor and in infants <1mo, there are no well-documented cases of hemolytic reactions in neonates. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

The long clinical experience is reassuring, though the literature is conflicting. One study whose subjects received 100mg concluded nitrofurantoin is actively transported into human milk, and that a nursing newborn could ingest 6% of the maternal dose. Another study whose subjects received 50mg found a much lower M:P ratio and concluded the likelihood of a nursing newborn ingesting a clinically relevant amount of nitrofurantoin was low. Thus, concern remains for Breastfeeding women treated therapeutically with nitrofurantoin if they have a family history of G6PD deficiency or sensitivity to nitrofurantoin.

Pregnancy

. Hypertension during pregnancy: Hypertension remains a significant cause of maternal and fetal morbidity and death. Severe hypertension during

Pregnancy

(BP >170/110mmHg) should be treated immediately to improve both maternal and fetal outcome. An uncontrolled reduction in BP may lead to coma, stroke, MI, 794 acute renal failure, and death. Treatment of a hypertensive episode during

Pregnancy

further complicates the process because an acute decrease in BP might adversely affect the fetus. Thus, the goal is not just to decrease BP, but to do so with minimal adverse effects while preserving organ function. It is suggested NO donors may have a therapeutic role in preeclampsia. Doppler studies are conflicting. Some investigators report vascular smooth muscle sensitivity to nitroglycerin is unaltered by preeclampsia, while others observe that nitroglycerin produces a more profound decrease in BP of preeclamptic women compared to normal subjects. Nitroglycerin also causes a fall in the resistance indices of the uterine arteries whether administered acutely or chronically. It is unknown whether the decline in resistance is associated with an increase in perfusion. Low-dose prophylactic nitroglycerin beginning in the 2nd trimester does not reduce the incidence of preeclampsia or IUGR. Cervical ripening and tocolysis: The NO-cGMP relaxation pathway is present in the human cervix and uterus and it has been postulated NO may have a physiologic role in uterine quiescence and cervical ripening. High doses of sublingual or IV nitroglycerin have been used acutely as a uterine relaxant to assist fetal surgery, fetal extraction at cesarean section, external version, internal intrapartum podalic version of the 2nd twin, manual exploration of the uterus to remove a retained placenta, and replacement of an inverted uterus. Yet placebo-controlled trials demonstrate nitroglycerin is no better than placebo for the facilitation of fetal extraction at cesarean section, or for external version. IV nitroglycerin currently continues to be used intra- and postoperatively to facilitate uterine relaxation during or after open uterine fetal surgery. Pulmonary edema is the most common complication. The short t/2 (2.5min) of nitroglycerin makes long-term therapy difficult, and tolerance is associated with longer acting donors. Nitroglycerin has also been used for intrapartum management of fetal distress. In a recent RCT, there was no difference between nitroglycerin and terbutaline in successful acute intrapartum fetal resuscitation. However, terbutaline provided more effective tocolysis with less impact on maternal BP. There are no identifiable placebo-controlled trials of intrauterine resuscitation. While nitroglycerin reduces the force necessary to dilate the cervix for a 1st trimester termination, it is less effective than prostaglandins for cervical ripening. Nitroglycerin has also proved a poor tocolytic. It does not inhibit uterine contractility in sheep. In laboring women, a 800mcg/dose reduces BP but has no effect on either uterine tone or contractility. Controversy continues regarding the ability of nitroglycerin to prevent preterm labor. Nitroglycerin is more effective than placebo but similar to a b-agonist or magnesium sulfate as a tocolytic agent. Its purported ability to delay labor was gestational age dependent.

Breastfeeding

There is no published experience in nursing women. It is unknown whether nitroglycerin enters human breast milk. However, considering the indication, dosing, and clearance rate, limited nitroglycerin use is unlikely to pose a clinically significant risk to the

Breastfeeding

neonate.

Pregnancy

. The metabolism of nitroprusside is important to remember. One molecule of nitroprusside combines with Hb to produce 1 molecule of cyanmethemoglobin and 4 CN?ions. Thiosulfate reacts with cyanide to produce thiocyanate. Thiocyanate is eliminated in the urine. Cyanide not otherwise removed binds to cytochromes. Cyanide is much more toxic than methemoglobin or thiocyanate. Hypertension during pregnancy: Hypertension remains a significant cause of maternal and fetal morbidity and death. Severe hypertension during

Pregnancy

(BP >170/110mmHg) should be treated immediately to improve both maternal and fetal outcome. An uncontrolled reduction in BP may lead to coma, stroke, MI, acute renal failure, and death. Treatment of an acute hypertensive episode during

Pregnancy

further complicates the process because an acute decrease in BP might adversely affect the fetus. Thus, the goal is not just to decrease BP, but to do so with minimal adverse effects while preserving organ function. It has been suggested NO donors could have a therapeutic role in preeclampsia. IV nitroprusside is an excellent hypotensive agent with the added advantage of a titratable effect. Nitroprusside exerts its relaxant effect by an endothelium-independent mechanism. Pharmacologic studies reveal that in vitro vasorelaxation in response to nitroprusside is attenuated in vessels obtained from preeclamptic women. Conversely, many severely preeclampsia patients are relatively or absolutely hypovolemic. In these patients, systemic BP may be extremely sensitive to small doses. Therefore, some clinicians begin therapy at lower rates of infusion (e.g., 0.5-0.1mcg/min). Cervical ripening: The NO-cGMP relaxation pathway is present in the human and cervix uterus. Nitroprusside decreases collagen cross-links in the guinea pig cervix. It reduces the force necessary to dilate the cervix for a 1st trimester termination.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether nitroprusside crosses the human placenta. Nitroprusside dilates the fetal vascular bed of the isolated perfused placenta, and its efficacy is unaffected by preeclampsia or IUGR. Fetal cyanide toxicity occurs in sheep after maternal administration. It is reversed by maternal administration of sodium thiosulfate, which unfortunately does not cross the human placenta. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether nitroprusside enters human breast milk. However, considering the indication, dosing, and clearance rate, limited nitroprusside use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Gastroesophageal reflux and heartburn are reported by 45-85% of women during pregnancy. There are no adequate reports or well-controlled studies of nizatidine in pregnant women. Nizatidine should be reserved for patients with severe symptoms.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether nizatidine crosses the human placenta in vivo. It freely crosses the isolated perfused cotyledon. A collaborative study by the European Network of Teratology Information Services of H2blockers noted an excess of preterm deliveries in the exposed group. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Nizatidine is scantly excreted into human breast milk. On average, <0.1% of the maternal dose is secreted during a 12h interval after either single or multiple doses. This is less than either cimetidine or ranitidine. Thus, it is unlikely the Breastfeeding newborn would ingest a clinically relevant quantity. The relevance of the observation that pups reared by nizatidine- treated lactating rats had poor growth is unclear.

Pregnancy

. Norethindrone is the progestogen in several popular oral contraceptives. The use of oral contraceptives containing norethindrone is causally related to an increased incidence of breakthrough bleeding. A slight increase in the incidence of ectopic

Pregnancy

may occur with progesterone-only contraceptives. There is no indication for norethindrone during

Pregnancy

and lactation.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Norethindrone likely crosses the human placenta since there are scattered cases of masculinized female fetuses reported. Most consist of clitoral hypertrophy not requiring surgical treatment. 1st trimester exposure is an indication for a detailed anatomic ultrasound between 18 and 22w. Norethindrone is not teratogenic in rodents.

Breastfeeding

Small amounts of norethindrone pass into the breast milk, resulting in steroid levels of 1-6% that of maternal plasma in the infant. Long- term follow-up studies reveal that progestogen-only contraceptives do not adversely affect Breastfeeding and infant development.

Pregnancy

. There are no adequate reports or well-controlled studies of norfloxacin in pregnant women (see Ciprofloxacin).

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether norfloxacin crosses the human placenta. The limited human experience is reassuring, as 1st trimester use does not appear to be associated with an increased risk of malformations or musculoskeletal problems. Animal studies (rodent, monkey) are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses 6-50higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether norfloxacin enters human breast milk.

Pregnancy

. Norgestrel is a synthetic progestogen that, alone or in combination with estrogen, is used in several popular oral, SR, and local (IUD) forms of contraception. It is pharmacologically similar to levonorgestrel. Progestin-only emergency contraception (1 tab PO q12h ?2) is available as a prepackaged product. The levonorgestrel-only regimen prevents 85% of unintended pregnancies compared with 57% for the Yuzpe regimen (2 tab each of 50mcg ethinyl estradiol and 0.25mg levonorgestrel, repeated 12h later). Though the implantable form (Norplant) is effective, patient acceptance is poor with up to 65% reporting menstrual abnormalities; 7.5% discontinue use in less than 4y because of increased bleeding. Other Side effects include acne, hirsuitism, weight gain, headache, breast tenderness, N/V, thromboembolism, MI, hypertension, hepatic 804 adenoma, edema, breakthrough bleeding, altered menstrual bleeding, amenorrhea, melasma, rash, and dizziness.

Fetal Health

There are no adequate reports or well-controlled studies of norgestrel in human fetuses. In utero exposure of male fetuses to progestational agents may double the risk of hypospadias. While there are insufficient data to quantify the risk for the female fetus, some progestational agents may cause mild virilization of the external genitalia. Defects outside the external genitalia are not reported in either humans or rodents. 1st trimester exposure is an indication for a detailed anatomic ultrasound between 18 and 22w. Breastfeeding Norgestrel is excreted into maternal milk. Maintaining a time interval between mini-pill intake and

Pregnancy

. Depression is common during and after pregnancy, but typically goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. There are no adequate reports or well-controlled studies of nortriptyline in pregnant women. Women who experienced one episode of postpartum-onset major depression are at high risk for subsequent recurrence. Unfortunately, nortriptyline is no different than placebo as prophylaxis for the prevention of recurrent postpartum depression in a high-risk population. Cigarette smoking during

Pregnancy

is the single largest modifiable risk for pregnancy- related morbidity and death in the US. Although NRT (gum, patch, nasal spray, and inhaler) combined with bupropion has the highest rate of success, nortriptyline also has a positive impact on smoking cessation rates. Nortriptyline is used for the treatment of neuropathic pain, chronic pain, and panic disorder. Its use for these indications may be avoidable during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Maternal and umbilical cord sera were collected at delivery from 10 women taking nortriptyline. The F:M ratios of nortriptyline and its active metabolite, cis-10-hydroxynortriptyline, were 0.68 ? 0.40 and 1.40 ? 2.40, respectively. Fetal exposure may be limited because of its lipophilicity. A case report suggested an association between nortriptyline and limb anomalies. There is no other support for this possibility. Rodent teratogenicity studies have yielded conflicting results.

Breastfeeding

Nortriptyline is excreted at low concentration into human breast milk. It is estimated the newborn would ingest only 2.5% of the corresponding maternal weight-corrected dose. Not surprisingly, nortriptyline levels are typically at or below the level of detection in the nursing newborn. Nortriptyline is generally considered a drug of choice for Breastfeeding women suffering from depression. 806

Pregnancy

. There are no adequate reports or well-controlled studies of novobiocin in pregnant women. Novobiocin should be used only after other antibiotics with lower toxicity have failed. 807

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether novobiocin crosses the human placenta. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether novobiocin enters human breast milk. Studies in animals (cows, mice) report novobiocin is excreted into breast milk and can be used to treat bovine mastitis.

Pregnancy

. Candida vaginitis is perhaps the most common female genital tract infection. Nystatin is an antifungal antibiotic that is both fungistatic and fungicidal in vitro against a wide variety of yeasts and yeastlike fungi. It is a polyene antibiotic obtained from 808 Streptomyces noursei. The vaginal milieu during

Pregnancy

predisposes to C. albicans overgrowth. In vitro, nystatin is highly effective against 83% of sensitive strains of tested C. albicans. There are no adequate reports or well-controlled studies of nystatin in pregnant women. It is not clear whether the various imidazole compounds differ in efficacy for mycotic vaginitis. Nystatin is thought less effective than miconazole for the treatment of vaginal candidiasis during pregnancy, though there are no randomized trials to substantiate this conclusion. There is no significant difference in the cure rates achieved after 7d or 14d of therapy. More patients relapsed after a cure with nystatin than with miconazole.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether nystatin crosses the human placenta. 1st trimester use of nystatin (and imidazole agents) is unassociated with an increased prevalence of spontaneous abortion or fetal malformation. Congenital candidiasis of the neonate?s skin rarely occurs, and nystatin is used to treat this infection and avoid septicemia. Rodent teratogenicity studies are limited to a single report where fetal losses were associated with maternal toxicity.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether nystatin enters human breast milk. However, considering the indication and dosing, limited nystatin use is unlikely to pose a clinically significant risk to the Breastfeeding neonate. Nystatin is not effective treatment of nipple candidiasis.

Pregnancy

. There is no published experience with topical oatmeal during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies of topical oatmeal in human fetuses. Absorption is likely insignificant.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. As a traditional food substance, oatmeal is unlikely to pose a clinically significant risk to the nursing infant.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Octreotide has pharmacologic actions that mimic the natural hormone somatostatin, but is more potent. There are multiple case reports of octreotide use during

Pregnancy

without obvious adverse effect, typically for the treatment of acromegaly. Depressed vitamin B12levels and abnormal Schilling tests are observed in some patients, and monitoring of vitamin B12is recommended. Octreotide reportedly improves implantation in supraovulated mice.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is not known whether octreotide crosses the human placenta. It does not affect placental GH production. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Octreotide enters human breast milk, but the reported concentrations are unlikely to have a clinically significant effect on the nursing infant.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Ofloxacin achieves high tissue penetration. It is not effective prophylaxis for infection after therapeutic abortion; doxycycline is preferred. The FDA has added a black box warning covering the potential for tendon rupture.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Less than 4% of maternal ofloxacin crosses the isolated perfused human placenta, though clearance is such that potentially therapeutic levels in AF and sera make it a candidate for fetal therapy if otherwise safe. In humans, fluoroquinolones are not associated with an increased risk of malformation. Neither ophthalmic nor otic application results in significant systemic drug levels. In general, rodent studies are reassuring, though some rodent models using otic application revealed minor skeletal abnormalities and IUGR. The administration of very high multiples of the MRHD is associated with fetal toxicity. 812

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Ofloxacin achieves an M:P ratio of ?1 but is consistently lower than ciprofloxacin. Serum and milk were obtained from 10 women simultaneously at 2, 4, 6, 9, 12, and 24h after ofloxacin. The mean breast milk levels were 2.4, 1.9, 1.3, 0.6, 0.3, and 0.05mcg/ml, respectively. Even with 100% oral absorption, Breastfeeding mothers who take ofloxacin will expose their infants to ofloxacin concentrations below that being studied in the pediatric population.

Pregnancy

. Olanzapine is an atypical antipsychotic agent whose clearance is 30% lower in women. However, effectiveness or Side effects include hypotension, tachycardia, menstrual irregularities, hyperprolactinemia, tardive dyskinesia, extrapyramidal symptoms, diabetes mellitus, hyperglycemia, somnolence, weight gain, constipation, dry mouth, dyspepsia, rhinitis, fever, and elevated LFTs.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. In one study, the mean F:M ratio was variable but overall quite high (72.1%; standard deviation [SD] = 42.0%); it was only about 33% in a second report. This contrasts with quetiapine (mean = 23.8%, SD = 11.0%). There were tendencies toward higher rates of low birth weight (30.8%) and NICU admission (30.8%) among neonates exposed to olanzapine. The

Pregnancy

outcomes of women who contacted a teratogen information service after exposure to olanzapine appeared normal. As for most psychotropic drugs, monotherapy and the lowest effective quantity given in divided doses to minimize the peaks can minimize the risks. Rodent studies are reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. Embryo and fetal toxicities were seen with high doses. There was no effect of intrauterine exposure on postnatal learning. 814 Breastfeeding There are no adequate reports or well-controlled studies in nursing women. Olanzapine enters human breast milk, though the kinetics remain to be defined.

Pregnancy

. The published experience with olmesartan during

Pregnancy

is limited to a case report noting perinatal renal impairment. The lowest effective dose should be used when olmesartan is absolutely required during

Pregnancy

for BP control.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Olmesartan probably crosses the human placenta. Inhibitors of the renin-angiotensin system as a group cross the human placenta. Adverse fetal effects are reported for the class of drugs across gestation and include cranial hypoplasia, anuria, reversible or irreversible renal failure, death, oligohydramnios, prematurity, IUGR, and PDA. The available case report suggets this is true for olmesartan. In those rare instances when these inhibitors are necessary, women should be apprised of the potential hazards and serial ultrasound examinations conducted. If oligohydramnios is detected, olmesartan should be discontinued unless lifesaving for the mother, and antenatal surveillance initiated. Oligohydramnios may not appear until after irreversible injury. Neonates with in utero exposure should be closely observed for hypotension, oliguria, and hyperkalemia.

Breastfeeding

There is no published experience in nursing women. It is unknown whether olmesartan enters human breast milk, though it is secreted at low concentration in rat milk.

Pregnancy

. There is no published experience with olopatadine during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether olopatadine crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Very high multiples of the MRHD are associated with fetal toxicity.

Breastfeeding

There is no published experience in nursing women. It is unknown whether olopatadine enters human breast milk, though it has been found in rodent milk. However, considering the dose and route, it is unlikely nursing could result in a clinically significant level in the neonate.

Pregnancy

. There are no adequate reports or well-controlled studies of olsalazine in pregnant women. Limited published experience consists predominantly of case reports and small series. It suggests that olsalazine retains efficacy during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Limited quantities of olsalazine and its metabolites cross the human placenta. Epidemiological study is reassuring. Rodent studies conducted at multiples of the MRHD revealed IUGR and delayed skeletal and organ maturation.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. In a single study, neither olsalazine nor its main active metabolite was detected in breast milk up to 48h after ingestion. However, oral administration to lactating rats in doses 5-20the MRHD reduced growth in the pups.

Pregnancy

. Omeprazole is effective treatment for a number of hypersecretory disorders, and effective preoperative prophylaxis (20-40mg PO qd) against aspiration pneumonitis. While there are no adequate reports or well-controlled studies in pregnant women, omeprazole appears to retain its efficacy during pregnancy. Though it increases human myometrial contractility in isolated muscle strips, there are no reports of an increased prevalence of preterm delivery. Omeprazole is advocated to lower gastric pH prior to cesarean section, but the results of the randomized trials are inconsistent, perhaps reflecting dose and route of delivery. Further, it and similar agents require 20-30min to take effect. Thus, Bicitra (citric acid/sodium citrate solution), perhaps with metoclopramide to enhance lower esophageal sphincter tone, remain agents of choice for emergent procedures.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether omeprazole crosses the human placenta. Proton pump inhibitors in general, and omeprazole specifically, are not associated with an increased risk of malformations. In the ewe, the F:M ratio approximates 0.5 and is strongly related to the rate of maternal clearance. Rodent studies are generally reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. However, embryo and fetal toxicity are noted in some models when multiples of the MRHD are used.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Omeprazole enters human breast milk, but milk concentrations are less than 10% of the maternal serum level. Thus, the nursing infant is unlikely to ingest a clinically significant amount.

Pregnancy

. Ondansetron is effective for N/V of pregnancy, but the published experience is inadequate to yet consider it first-line therapy. A single IV dose (4mg) given prophylactically significantly reduces the N/V after cesarean delivery, though the same may be accomplished with other less expensive antiemetic agents. Since ondansetron (0.1mg/kg IV ?1) significantly reduces the pruritus associated with intrathecal morphine or fentanyl, some clinicians choose this agent as their antiemetic of choice no matter what the cost; others use less expensive alternative agents. It is no better than metoclopramide as prophylaxis for N/V after minor gynecologic surgery, but superior to it for patients undergoing chemotherapy. Recent study indicates that epidural ondansetron 820 is more effective preventing intrathecal morphine?associated post?cesarean section pruritus and nausea than IV ondansetron. However, it is apparently not effective when given IV for prophylaxis when fentanyl is used during labor.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is not known whether ondansetron crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether ondansetron enters human breast milk. It is detectable in rat milk.

Pregnancy

. Oprelvekin is genetically engineered IL-11. There is no published experience with it during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. IL-11 is an endogenous cytokine with many actions and interactions. Oprelvekin is embryocidal in some rodents at doses analogous to those used in humans. IUGR and reduced ossification are also reported.

Breastfeeding

There is no published experience in nursing women. It is unknown whether oprelvekin enters human breast milk.

Pregnancy

. Orlistat is a reversible lipase inhibitor for obesity management that acts by inhibiting the absorption of dietary fats. It is also an antiangiogenic agent with a novel mechanism of action: orlistat prevents the display of vascular endothelial growth factor (VEGF) receptor (VEGFR2/KDR/Flk1) on the endothelial cell surface. There is no published experience with it during pregnancy. It has 822 been suggested but unproven that orlistat might interfere with the absorption of oral contraceptives and thus diminish their efficacy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether orlistat crosses the human placenta. However, the mother absorbs little systemically (peak plasma levels at the limit of detection). Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Some dilation of the cerebral ventricles was noted.

Breastfeeding

There is no published experience in nursing women. Considering the maternal systemic level, it is unlikely a clinically relevant concentration of orlistat enters human breast milk. It is not known whether the milk components are altered.

Pregnancy

. There is no published experience with orphenadrine during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether orphenadrine crosses the human placenta. There is some passage across the ovine placenta. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There is no published experience in nursing women. It is unknown whether orphenadrine enters human breast milk.

Pregnancy

. There is no published experience with oseltamivir during pregnancy. Evidence of evolving viral resistance is emerging. Prophylaxis is not a substitute for vaccination (CDC Immunization Practices Advisory Committee).

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Oseltamivir does not apparently cross the human placenta. Even when the isolated cotyledon is perfused at 600-800 times the normal plasma level, the clearance index was only 0.13. Rodent studies are reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. Maternal toxicity is noted along with a nonsignificant increase in skeletal abnormalities.

Breastfeeding

There is no published experience in nursing women. It is unknown whether oseltamivir enters human breast milk. 824

Pregnancy

. Oxacillin is penicillinase-resistant, acid-resistant, semisynthetic penicillin suitable for oral administration. There is a long clinical experience with oxacillin during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Most penicillin compounds cross the human placenta. There is no evidence oxacillin is teratogenic in humans after a long clinical experience. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. There are a number of interesting studies in rodents suggesting in utero exposure alters in utero and postnatal immune responses. The implications are unclear.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Oxacillin is concentrated in human breast milk 825 exceeding the typical MIC, making it suitable for the treatment of puerperal mastitis. Unfortunately, many staphylococci are now resistant. Though it is generally considered compatible with breastfeeding, clindamycin is a better selection.

Pregnancy

. Oxaprozin is an NSAID with anti-inflammatory, analgesic, and antipyretic properties. There is no published experience with oxaprozin during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether oxaprozin crosses the human placenta. Other NSAIDs cross the human placenta and are associated with decreased fetal urination and ductal constriction. Malformed fetuses were observed in rabbits but not mice treated 826 with doses analogous to the human. Pup survival was also reduced.

Breastfeeding

There is no published experience in nursing women. It is unknown whether oxaprozin enters human breast milk. It does enter rodent milk.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Alcoholism is an often-unrecognized problem during

Pregnancy

that poses a clear hazard to mother and child. Oxazepam has a wide safety range compared to other benzodiazepines. Some also consider oxazepam a second-line agent for the treatment of pruritus during pregnancy, despite the lack of study for this indication. It is highly effective for the short-term relief of anxiety. Physical and psychological dependency is a risk with chronic usage.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Oxazepam crosses the human placenta at a slower rate than diazepam, reaching an F:M ratio during the 1st trimester of 0.5 after 4h. The impact of benzodiazepines in human

Pregnancy

appears in general to have been overestimated. Long-term follow-up studies are for the most part reassuring. Fetal exposure can be minimized by qid dosing to reduce peak levels. Subtle behavioral affects of in utero oxazepam exposure are reported in rodents.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Oxazepam enters human breast milk in low concentrations unlikely to be clinically significant for the Breastfeeding infant.

Pregnancy

. Oxcarbazepine is the 10-keto analogue of carbamazepine and thus an enzyme-inducing agent. Either a higher dose oral contraceptive or a second method of contraception is recommended. Planned

Pregnancy

and counseling on the importance of folate supplementation and medication adherence are important. There are no adequate reports or well-controlled studies in pregnant women. Maternal levels do decline with advancing gestation, suggesting the need for a dose adjustment. Vitamin K (10mg qd) is recommended for the last 4w of gestation in women taking enzyme-inducing agents such as carbamazepine, oxcarbazepine, phenobarbital, phenytoin, and topiramate.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Oxcarbazepine crosses the human placenta, reaching an F:M ratio approximating unity with the placenta taking an active role in its metabolism. The frequency of neonatal bleeding complications is not increased, calling into question the necessity of vitamin K supplementation. Oxcarbazepine is closely related structurally to carbamazepine, which is considered teratogenic in humans. Polytherapy increases the risk. If feasible, the number of agents used during

Pregnancy

should be reduced. Rodent studies performed at doses analogous to the human demonstrate embryo lethality, IUGR, and a variety of malformations (craniofacial, CV, and skeletal).

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Though the concentrations of oxcarbazepine 829 and its major metabolites in human breast milk are low, and neonatal concentrations decline despite breastfeeding, periodic monitoring of the infant concentration is suggested by some.

Pregnancy

. There is no published experience with oxiconazole during pregnancy. However, <1% of the applied dose is absorbed systemically.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether oxiconazole crosses the human placenta. However, the maternal systemic concentration is not likely to reach a clinically relevant level. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether oxiconazole enters human breast milk. Because <1% of the applied dose is absorbed systemically, it is unlikely the Breastfeeding newborn would absorb a clinically relevant amount.

Pregnancy

. Oxtriphylline is the choline salt of theophylline. Its clearance is increased in cigarette smokers, in patients with CHF and hepatic dysfunction, and in those taking a variety of other drugs such as cimetidine, erythromycin, lithium, oral contraceptives, and phenytoin. There is no published experience with oxtriphylline during pregnancy. See Theophylline.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether oxtriphylline crosses the human placenta. Rodent studies have not been conducted. See Theophylline.

Breastfeeding

There is no published experience in nursing women. While it is unknown whether oxtriphylline enters human breast milk, theophylline is distributed into breast milk and may cause irritability or other signs of toxicity in nursing infants (see Theophylline).

Pregnancy

. There is no published experience with oxybutynin during pregnancy. 832

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is not known whether oxybutynin crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether oxybutynin enters human breast milk.

Pregnancy

. Oxychlorosene is used as a topical antiseptic for treating localized infections, particularly when resistant organisms are present. The greatest published experience is for the treatment of interstitial cystitis. However, it has also proved useful for wound 833 de?bridement to promote secondary healing. There are no adequate reports or well-controlled studies of oxychlorosene in pregnant women. Any systemic absorption is likely minimal.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether oxychlorosene crosses the human placenta. Any systemic absorption is likely minimal.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether oxychlorosene enters human breast milk. Any systemic absorption of hypochlorous acid is likely minimal.

Pregnancy

. Thirty milligrams (30mg) of oxycodone is approximately equal to 10mg morphine. Oxycodone is not intended for use as a prn analgesic. Women have, on average, plasma oxycodone concentrations up to 25% higher than men on a body-weight- adjusted basis. In one RCT, the oxycodone-acetaminophen combination provided superior pain control after cesarean delivery with fewer Side effects include dependency, hepatotoxicity, seizures, respiratory depression, dizziness, sedation, N/V, pruritus, rash, dysphoria, and constipation. 834

Fetal Health

There are no adequate reports or well-controlled studies of oxycodone in human fetuses. Other drugs in its class readily cross the human placenta. Oxycodone abuse during

Pregnancy

may be associated with neonatal withdrawal. Breastfeeding Oxycodone was detected in the milk of mothers who have taken any dose in a 24h period, with significant correlation between maternal plasma and milk levels (r2=.81). The M:P ratio was 3.2:1. Over the next 48h, the relationship between plasma and milk levels was weaker (r2=.59). Oxycodone levels up to 168ng/ml were detected in breast milk (20% >100ng/ml), though it was detected in only 1/41 infants tested. Maternal oxycodone intake up to 72h post?cesarean section poses only minimal risk to the

Pregnancy

. Allergic rhinitis affects about1=3 of reproductive-age women. Oxymetazoline is available OTC, and the prevalence of its use during

Pregnancy

and lactation are unknown. Chronic abuse may lead to rebound rhinitis. Because there are no adequate reports or well-controlled studies in pregnant women, it should be considered a second-line agent behind 1st generation antihistamines such as chlorpheniramine. Oxymetazoline binds to human myometrium, and can in vitro cause contraction of both the myometrium and the umbilical artery. Preeclamptic women may experience an acute rise in BP after administration.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is suggested that some vasoactive decongestants may be involved in the etiology of gastroschisis, including oxymetazoline. It can also constrict the umbilical artery, and is suggested as a cause of a nonreactive NST. However, another study of healthy pregnancies could detect no effect of oxymetazoline on fetal Doppler flows in a variety of vessels.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether oxymetazoline enters human breast milk. However, considering the dose, route, and frequency, it is unlikely the Breastfeeding neonate would absorb clinically relevant quantities.

Pregnancy

. Oxymorphone was at one time popular for labor analgesia. It provides similar pain relief with less pruritus compared to morphine when used with epidural analgesia. Oxymorphone is an alternative to morphine administered by PCA after cesarean section, but may be associated with an increase in nausea. The level of sedation is similar.

Fetal Health

There are no adequate reports or well-controlled studies of oxymorphone in human fetuses (see Morphine).

Breastfeeding

There is no published experience in nursing women. It is unknown whether oxymorphone enters human breast milk. Only limited quantities of morphine enter breast milk.

Pregnancy

. When penicillin is contraindicated, tetracyclines are alternative drugs for the treatment of N. gonorrhoeae, T. pallidum and T. pertenue (syphilis and yaws), Listeria monocytogenes, Clostridium species, B. anthracis, Fusobacterium fusiforme (Vincent?s infection), and Actinomyces species. There are no adequate reports or well-controlled studies of oxytetracycline in pregnant women. Tetracyclines are generally considered contraindicated during

Pregnancy

because of their effect on the fetal teeth.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Oxytetracycline rapidly crosses the placenta and blood-brain barrier. Epidemiologic study links 1st trimester use of oxytetracycline with NTDs, cleft palate, and CV malformations. Tetracyclines in general are known to cause tooth discoloration when given in the 2nd half of

Pregnancy

and during the neonatal period. They are incorporated into fetal bones in a reversible fashion. Rodent studies are reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. However, oxytetracycline produced dose-dependent maternal and embryo toxicity. 838

Breastfeeding

There is no published experience in nursing women. It is unknown whether oxytetracycline enters human breast milk. Other tetracyclines are excreted in breast milk.

Pregnancy

. The physiologic role of oxytocin in the stimulation and maintenance of human labor remains unclear. Though the search continues for new oxytocin receptor antagonists, large trials conducted with one antagonist revealed it was at best no better than many of the tocolytic agents already available. Oxytocin is usually effective stimulating rhythmic uterine contractions and is the drug of choice for induction 839 and augmentation of labor. In some geographic locales, an OCT is still used to assess placental reserve in the at-risk pregnancy. It is unclear whether routine amniotomy enhances the efficacy of oxytocin. High-dose oxytocin (4.5mIU/min initially, increased by 4.5mIU/min q30min) is associated with significantly shorter labors without demonstrable adverse fetal or neonatal effect compared to a low-dose oxytocin (1.5mIU/min initially, increased by 1.5mIU/min q30min) protocol. In VBAC patients, there is a dose-response relationship between the maximum oxytocin infusion rate and uterine rupture. Added caution is indicated at the higher doses of oxytocin during a VBAC attempt. Low-dose oxytocin (1-4mIU/ min) is equivalent to misoprostol for cervical ripening. Oxytocin is also important for the management of postpartum bleeding. Oxytocin infused at 80mIU/500ml over 30min for the first 30min postpartum reduces the need for additional uterotonic agents after cesarean delivery compared to an infusion of 10mIU/ 500ml over 30min at cord clamping. While it is often given (10mIU IV) with the delivery of the anterior shoulder, there is no clinical advantage to its administration then compared to after placental delivery for the reduction of 3rd stage hemorrhage. Injection into the umbilical vein after delivery has little impact on the 3rd stage of labor.

Fetal Health

Oxytocin is used only to end pregnancy, and as such poses only labor-associated risks to the fetus. There are no indications for its use in the 1st trimester, and animal teratogen studies have not been conducted. Electronic FHR monitoring is indicated for all antepartal infusions.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Endogenous oxytocin is essential for the initiation of lactation, and synthetic oxytocin can aid the establishment of a milk reflex.

Pregnancy

. Paclitaxel is a natural product. It is usually combined with cisplatin as first-line therapy. There are dozens of women given paclitaxel during pregnancy. In one, the median maternal age was 36y (range: 30-42y), and the primary site was ovarian in 5 (four carcinomas and one dysgerminoma) and the breast in 4. Paclitaxel began during the 2nd trimester in 4 instances, and during the 3rd trimester in the remaining 5. No malformations were reported, and the offspring seemed healthy with a median follow-up of 16mo (range: 3-36mo). Only one team studied the pharmacokinetics of paclitaxel (175mg/m2IV over 3 h) during pregnancy. The Cmaxand AUC of paclitaxel were decreased compared with nonpregnant patients. The estimated clearance, t/2, and volume of distribution were each within the ranges previously reported for nonpregnant patients.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether paclitaxel crosses the human placenta. However, several case reports note the development of oligohydramnios during paclitaxel therapy. Rodent studies reveal embryotoxicity and IUGR, but no teratogenicity.

Breastfeeding

There is no published experience in nursing women. It is unknown whether paclitaxel enters human breast milk. It is concentrated in rat milk.

Pregnancy

. There are no adequate reports or well-controlled studies of pamidronate in pregnant women. The published experience consists of several case reports. In one, pamidronate was employed in the 3rd trimester to treat hypercalcemia secondary to metastatic breast carcinoma. There was no apparent adverse effect. In another, a woman with metastatic breast cancer was treated at 28w after unsuccessful chemotherapy, deteriorating renal function, frequent contractions, and a calcium level of 17.6mg/dl. Pamidronate dramatically decreased both the calcium levels and the frequency of uterine contractions. In six other instances, women with either polyostotic fibrous dysplasia or osteogenesis imperfecta were treated before conception and throughout

Pregnancy

without any apparent adeverse maternal 842 or fetal effects. In animal studies, pamidronate inhibits bone resorption at the recommended dose for hypercalcemia apparently without inhibiting bone formation and mineralization.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pamidronate crosses the human placenta. The limited human experience is reassuring. Indeed, pamidronate may represent an ameliorating fetal therapy for congenital osteogenesis imperfecta if there is placental transport. Rodent studies revealed maternal toxicity, presumably associated with hypocalcemia, and fetal skeletal retardation, but no evidence of teratogenicity. The delayed skeletal formation suggests pamidronate crosses the rodent placenta.

Breastfeeding

There are no reports or well-controlled studies in nursing women. In a single case report, pamidronate was not found in human breast milk after a single IV dose. Women with hereditary hyperphosphatasia, a rare bone disorder characterized by increased bone turnover, may develop symptomatic hypercalcemia during lactation.

Pregnancy

. The enzymes in pancrelipase act locally in the GI tract, where either they may be digested, or their constituents partially absorbed and subsequently excreted in the urine. Undigested enzymes are excreted in the feces. There is no published experience in

Pregnancy

though it no doubt has been used for the treatment of cystic fibrosis.

Fetal Health

There are no adequate reports or well-controlled studies of pancrelipase in human fetuses. The enzymes are not absorbed in a functional format and pose no risk to the fetus. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience with pancrelipase in nursing women. However, the enzymes are not absorbed systemically and are unlikely to enter human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of pancuronium in pregnant women. However, it has a long clinical experience for cesarean delivery. Pancuronium is approximately 1=3 less potent than vecuronium, though its duration is longer at equipotent doses. As compared to vecuronium, pancuronium is also vagolytic with accompanying tachycardia?unwanted in some adults but perhaps desired during fetal transfusion. Magnesium sulfate enhances the neuromuscular blockade, and reversal may be incomplete. Neuromuscular blockade is reversed by anticholinesterase agents such as edrophonium, neostigmine, and pyridostigmine.

Fetal Health

There are no adequate reports or well-controlled studies of pancuronium in human fetuses. There is minimal transport across the human placenta. Pancuronium is often used for fetal paralysis to facilitate intrauterine procedures (0.3-0.6mg IV or IM). Because it increases HR, pancuronium blunts the normal decline in cardiac output after fetal intravascular transfusion. Fetal paralysis modestly reduces oxygen consumption.

Breastfeeding

There is no published experience in nursing women. It is unknown whether pancuronium enters human breast milk. However, it is unlikely a significant amount would enter the breast milk given once for the described indications.

Pregnancy

. There are <60 reported cases during

Pregnancy

in the literature. Pantoprazole seems effective for the approved indications.

Fetal Health

There are no adequate report or well-controlled studies in human fetuses. It is unknown whether pantoprazole crosses the human placenta. The limited published experience does not raise an alarm. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience during lactation. It is unknown whether pantoprazole enters human breast milk; it is excreted into rodent milk.

Pregnancy

. Pantothenic acid (a.k.a. vitamin B5) is a water-soluble B vitamin. There are no adequate reports or well-controlled studies of pantothenic acid in pregnant women. Its level may decline modestly during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Pantothenic acid is actively transported across the placenta. Epidemiologically, maternal intake of pantothenic acid correlates with birth weight, birth length, and head circumference. However, it is not presently known whether maternal supplementation increases the fetal concentration. Supplementation reduces the incidence of NTDs in mice treated with valproate.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Pantothenic acid enters human breast milk, and the concentration in term milk correlates with maternal serum, dietary intake, and urinary excretion. Maternal serum levels may decline modestly during lactation without supplementation.

Pregnancy

. Paregoric is a mixture of opium powder (anhydrous morphine, 0.4mg/mL) and ethanol. Other ingredients include benzoic acid, camphor, and anise oil. Its main actions are to increase intestinal muscular tone and to inhibit normal peristalsis. Paregoric?s principle medicinal use is to control fulminant diarrhea. It is also an antitussive. Paregoric is sometimes confused with laudanum, because their chemical names are similar: camphorated tincture of opium (paregoric) vs. tincture of opium (laudanum). However, laudanum contains 10mg/ml of opium, 25more than paregoric. Confusion between the two drugs has led to overdose and deaths. The term ??paregoric?? should always be used instead of ??camphorated opium tincture,?? since the latter may be confused with laudanum. There are no adequate reports or well-controlled studies of paregoric in pregnant women. It does not delay or inhibit preterm labor. See Morphine.

Fetal Health

There are no adequate reports or well-controlled studies of paregoric in human fetuses. Rodent teratogenicity studies have not been conducted, though the large clinical experience is reassuring. Paregoric is used postnatally for the treatment of neonatal withdrawal. See Morphine.

Breastfeeding

There are no adequate reports or well-controlled studies of paregoric in nursing women (see Morphine).

Pregnancy

. Paricalcitol is a synthetic vitamin D analog. There is no published experience in pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether paricalcitol crosses the human placenta. The results of rodent studies are mixed. Sequelae may reflect hypocalcemia rather than the drug.

Breastfeeding

There is no published experience during lactation. It is unknown whether paricalcitol enters human breast milk.

Pregnancy

. Paromomycin closely parallels neomycin. It is poorly absorbed orally?nearly 100% is recoverable from the stool. There are no adequate reports or well-controlled studies in pregnant women. A single case report documents the successful treatment of giardiasis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether paromomycin crosses the human placenta. However, it is unlikely the maternal systemic concentration will reach a clinically relevant level.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether paromomycin enters human breast milk. However, it is generally considered compatible with Breastfeeding because of the poor oral absorption.

Pregnancy

. Depression is common during and after pregnancy, but typically goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. There are no adequate reports or well-controlled studies of paroxetine in pregnant women. About 2=3 of women taking SSRIs during

Pregnancy

for major depression must increase their dose to maintain efficacy. Women should not feel compelled to stop paroxetine when they become pregnant if therapy is indeed indicated. If, after receiving appropriate evidence-based information, they decide to stop, it should be tapered gradually to avoid the abrupt discontinuation syndrome. There is growing clinical experience with the use of paroxetine for the treatment of postpartum depression. Paroxetine is also effective for the treatment of menopause-associated hot flashes.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Paroxetine crosses the human placenta, achieving a mean F:M ratio approximating 0.5, a value significantly 852 lower than that observed with citalopram and fluoxetine. Neonatal withdrawal symptoms are documented. Epidemiologic studies are somewhat mixed and suggest confounding factors are at play. Some larger studies suggest an increase in CV malformations after 1st trimester exposure to paroxetine. The effect is however small, appears dose-dependent (only above a daily dose of 25mg) and the most recent large epidemiological study found no such association. However, the risks may not be only structural. In one follow-up study, blunted facial-action responses were observed among infants exposed prenatally to SSRIs, whereas both prenatal and postnatal exposure was associated with reduced parasympathetic withdrawal and increased parasympathetic cardiac modulation during recovery after an acute noxious event. Given that postnatal exposure via breast milk is extremely low and altered biobehavioral pain reactivity is not associated with levels of maternal reports of depression, these findings suggest possible sustained neurobehavioral outcomes beyond the newborn period. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Paroxetine is excreted into human breast milk with the highest concentrations in the hind milk. However, the levels are variable, and no breastfed child studied to date has had clinically relevant levels detected, suggesting paroxetine is a good selection for Breastfeeding women.

Pregnancy

. There is no published experience with pegfilgrastim in pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pegfilgrastim crosses the human placenta. Rodent studies reveal increased postimplantation resorption and abortion rates and IUGR often at doses in excess of that recommended and in association with maternal toxicity.

Breastfeeding

There is no published experience during lactation. It is unknown whether pegfilgrastim enters human breast milk.

Pregnancy

. Interferons bind to specific cell surface membrane receptors to initiate a complex sequence of intracellular events. Alfa interferons, including peginterferon alfa-2b, may cause or aggravate fatal or life-threatening neuropsychiatric, autoimmune, ischemic, and infectious disorders. Patients should be monitored closely with periodic clinical and laboratory evaluations. Therapy should be discontinued in women with persistently severe or worsening signs or symptoms. In many, but not all, instances, these disorders resolve after discontinuation. There is no published experience with peginterferon alfa-2b in pregnancy. Irregular menstrual cycles occurred in cynomolgus monkeys treated SC with doses in multiples of the MRHD.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether peginterferon alfa-2b crosses the human placenta. High doses of native interferon alfa-2b were associated with abortion in cynomolgus monkeys.

Breastfeeding

There is no published experience during lactation. It is unknown whether peginterferon alfa-2b enters human breast milk. Unlike HIV, Breastfeeding is not considered a risk for the newborns of HCV-infected women.

Pregnancy

. There is no published experience with pemirolast in pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pemirolast crosses the human placenta. However, considering the dose and route, it is unlikely the maternal systemic concentration would achieve a clinically relevant level. Rodent teratogenicity studies revealed skeletal abnormalities following the systemic administration of doses 20,000or more above the MRHD.

Breastfeeding

There is no published experience during lactation. It is unknown whether pemirolast enters human breast milk. However, considering the dose and route, it is unlikely the breastfed neonate will ingest clinically relevant amounts. It is concentrated in rodent milk. 857

Pregnancy

. Pemoline has a pharmacologic activity similar to other known CNS stimulants; however, it has minimal sympathomimetic effects. There are no adequate reports or well-controlled studies in pregnant women. It has been used to treat narcolepsy during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pemoline crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether pemoline enters human breast milk.

Pregnancy

. Hypertensive disorders complicate 5-10% of pregnancies and are a leading cause of maternal and perinatal morbidity and death. There are no adequate reports or well-controlled studies of penbutolol in pregnant women. The free fraction of penbutolol increases during

Pregnancy

because of altered protein binding.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether penbutolol crosses the human placenta. Other b-blockers are associated with IUGR and fetal/neonatal bradycardia. The former is dose-dependent and appears to reflect an excessive drop in maternal cardiac output. Other neonatal sequelae associated with b blockade include hypoglycemia and hyperbilirubinemia. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Fetal toxicity was noted.

Breastfeeding

There is no published experience in nursing women. It is unknown whether penbutolol enters human breast milk.

Pregnancy

. There is no published experience with penciclovir in pregnancy. There is little systemic absorption after topical application.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether penciclovir crosses the human placenta; it does apparently cross the rodent placenta. However, considering the dose and route, it is unlikely the maternal systemic concentration will reach clinically relevant levels. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether penciclovir enters human breast milk. However, considering the dose and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts. One report suggests it rapidly is excreted into and then cleared from rodent breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Penicillamine is contraindicated during

Pregnancy

except for the treatment of Wilson?s disease and some cases of cystinuria. The published experience is limited to case reports and small series. Recurrent abortions are common in women with untreated Wilson?s disease. Successful pregnancies and uneventful full-term delivery may occur with treatment and in presymptomatic patients.

Pregnancy

does not seem to have adverse effect on the clinical course of Wilson?s disease. Zinc, which induces intestinal cell metallothionein that binds copper and prevents its transfer into blood, may be a suitable adjunct or alternative therapy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Penicillamine apparently crosses the human placenta, since congenital cutis laxa and associated defects such as micrognathia, contractures, and CNS abnormalities are reported in neonates of treated women. Teratogenicity has otherwise not been reported in women receiving low-dose penicillamine and zinc sulfate. Penicillamine is teratogenic in rodents at doses 6? the MRHD. Adverse effects include skeletal deformities, cleft palate, and embryotoxicity.

Breastfeeding

There is no published experience in nursing women. It is unknown whether penicillamine enters human breast milk.

Pregnancy

. Penicillin G is typically given parenterally because it is unstable in gastric hydrochloric acid. Because it is given IV, higher tissue concentrations are achieved than with penicillin VK (phenoxymethylpenicillin). There is a long clinical experience with penicillin G during

Pregnancy

that is reassuring. Vaginal GBS colony counts fall rapidly after intrapartum penicillin G, which explains in part the effectiveness of chemoprophylaxis. It is as effective as cephalothin for the prevention of post?cesarean section infection.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Most penicillins cross the human placenta to some extent. Penicillin G is efficiently transferred across the horse placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only trace amounts of penicillin G enter human 862 breast milk. It is generally considered compatible with breastfeeding.

Pregnancy

. Benzathine penicillin G is slowly absorbed after IM injection and subsequently hydrolysed to benzylpenicillin. It is the drug of choice when prolonged low concentrations of benzylpenicillin are required, allowing for prolonged antibiotic action over 2-4w. There are no adequate reports or well-controlled studies in pregnant women. Benzathine penicillin G remains the drug of choice for syphilis during pregnancy. However, it should be noted that Bicillin C-R (contains 1.2 million U of benzathine penicillin G and 1.2 million units of procaine penicillin G) is not recommended for treating syphilis because it contains only half the recommended dose of benzathine penicillin G. Medication errors have occurred, and as a result changes in product packaging were made; specifically, the statement ??Not for the Treatment of Syphilis?? has been added in red text to both the Bicillin CR and Billin CR 900/300 syringe labels. There is some concern benzathine penicillin G may not prevent neurosyphilis, but the overall risk appears low. Partner notification is mandatory to prevent the spread of the disease. About 40% of patients experience a Jarisch-Herxheimer reaction; treated women should be warned of the possibility and monitored closely for the first 48h. Benzathine penicillin G-penicillin G suspension (Bicillin L-A) 2.4 million U IM is insufficient as sole therapy for group B streptococcal prophylaxis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Most penicillins cross the human placenta to some extent. The currently recommended dose of benzathine penicillin G is effective for preventing congenital syphilis in most settings, although some additional study regarding dose modification is needed. Azithromycin and ceftriaxone are potential alternatives for penicillin-allergic women, but there is insufficient data on efficacy, which limits their use in pregnancy. Rodent studies of benzathine penicillin G are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only trace amounts of benzathine penicillin G enter human breast milk. It is generally considered compatible with breastfeeding.

Pregnancy

. Procaine penicillin G is a combination of benzylpenicillin with the local anaesthetic agent procaine. It is slowly absorbed after IM administration and hydrolysed to benzylpenicillin and thus used to achieve prolonged but low concentrations of benzylpenicillin. The combination seeks to reduce the pain and discomfort associated with a large IM injection of penicillin. There are no adequate reports or well-controlled studies in pregnant women. Procaine penicillin G may be used in place of benzathine penicillin G for the treatment of syphilis, but has no medical advantage.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Most penicillins cross the human placenta to some extent. Procaine penicillin G should behave the same as benzathine penicillin G. The large clinical experience is reassuring, as are the rodent studies, which reveal no evidence of 865 teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only trace amounts of procaine penicillin G enter human breast milk. It is generally considered compatible with breastfeeding.

Pregnancy

. Penicillin VK is the orally active form of penicillin. It is less active than benzylpenicillin and is only appropriate in circumstances where high tissue concentrations are not required. There are no adequate reports or well-controlled studies in pregnant women. However, there is a long clinical experience that is reassuring.

Fetal Health

There are no adequate reports or well-controlled studies of penicillin VK in human fetuses. Most penicillins cross the human placenta to some extent. The large clinical experience is reassuring, as are the rodent studies, which reveal no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only trace amounts of penicillin VK enter human breast milk. It is generally considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of pentamidine in pregnant women. Withholding appropriate PCP prophylaxis can adversely affect maternal and fetal outcomes. PCP during

Pregnancy

may have a more aggressive course with increased morbidity and death. Maternal and fetal outcomes are poor. Treatment with sulfamethoxazole-trimethoprim may improve outcome compared to other therapies. Aerosolized pentamidine does not appear to pose a significant risk to pregnant health care workers.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. There are no published human reports of concern, and human placental transport of pentamidine across the isolated cotyledon is limited. Pentamidine crosses the rodent placenta and penetrates all fetal compartments. Rodent studies are in general reassuring, revealing embryotoxicity but no teratogenicity or IUGR.

Breastfeeding

There is no published experience in nursing women. It is unknown whether pentamidine enters human breast milk. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. Pentazocine is a potent analgesic; 30-45mg is equianalgesic to morphine 10mg and meperidine 75-100mg. There are no adequate reports or well-controlled studies in pregnant women. Pentazocine is a poor choice for labor analgesia because of greater maternal respiratory depression than the alternatives. Some patients receiving narcotics, including methadone, experience withdrawal symptoms since pentazocine is a weak narcotic antagonist.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Pentazocine crosses the human placenta. The addictive combination of pentazocine and tripelennamine (T?s and blues) remains popular in some locales. Infants of women who use T?s and blues throughout

Pregnancy

have interactive deficits and withdrawal similar to methadone-addicted newborns. In general, rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. A single study in hamsters suggested an increased risk of CNS malformations.

Breastfeeding

There is no published experience in nursing women. While it is unknown whether pentazocine enters human breast milk, the clinical experience is reassuring.

Pregnancy

. Barbiturates produce CNS mood alteration ranging from excitation to sedation to hypnosis and deep coma. As a sleep aid, barbiturates are of limited value beyond the short term as they lose effectiveness after 1-2w. There are superior agents that have less effect on the sleep cycle. There are no adequate reports or well-controlled studies of pentobarbital in pregnant women. Hypnotic doses do not impair uterine activity during labor.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Pentobarbital rapidly crosses the human placenta. The highest concentrations are found in placenta, liver, and brain. Its administration during labor can cause neonatal respiratory depression. Preterm infants are particularly susceptible, and resuscitation equipment should be available. Chronic use during the 3rd trimester can yield addicted neonates who have an extended withdrawal syndrome. Retrospective, case-control studies suggest a connection between barbiturates and an increased risk of fetal abnormalities. However, there are no such reports specifically for pentobarbital, and the rodent studies are reassuring. There is a single study suggesting a reduction in fertility.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only small amounts of pentobarbital enter human breast milk, and it is generally considered compatible with breastfeeding.

Pregnancy

. There is no published experience with pentosan polysulfate in pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Pentosan polysulfate does not appear to cross the human placenta and should pose little risk during pregnancy.

Breastfeeding

There are no published studies in nursing women. It is unknown whether pentosan polysulfate enters human breast milk.

Pregnancy

. There is no published experience with pentostatin during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pentostatin crosses the human placenta. The developing mouse allantois is quite sensitive to pentostatin, and interference with allantois development leads to embryo lethality. Late exposure in rodent

Pregnancy

is associated with neural tube, craniofacial, and limb defects.

Breastfeeding

There is no published experience during lactation. It is unknown whether pentostatin enters human breast milk.

Pregnancy

. Pentoxifylline and its metabolites improve the flow properties of blood by decreasing viscosity. It also inhibits TNF-a?induced complement C3 synthesis. Pentoxifylline is used with tocopherol to treat IVF patients with a thin endometrium. It also enhances sperm motility prior to IVF or IUI. It has even been used in a preliminary study to treat endometriosis related infertility. In rodents, long-term use is associated with the development of mammary fibroadenomas. There are no adequate reports or well- controlled studies during pregnancy. Clearance is unaltered by pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pentoxifylline crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity was noted.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Pentoxifylline enters human breast milk, achieving near unity with maternal plasma. It is perhaps wise to 873 avoid pentoxifylline while Breastfeeding because of its association with mammary fibroadenomas in rodents.

Pregnancy

. Pergolide is effective primary treatment for pituitary macroprolactinomas. It is 10-1000more potent a dopamine 874 agonist than bromocriptine. There are no adequate reports or well-controlled studies in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pergolide crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether pergolide enters human breast milk. The pharmacologic action of pergolide suggests it may interfere with lactation, and thus should be avoided at least until the milk reflex is well established.

Pregnancy

. There is no published experience with perindopril during pregnancy. The lowest dose effective should be used when it is required during

Pregnancy

for BP control.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether perindopril crosses the human placenta. It does cross the rabbit placenta. Other renin-angiotensin system inhibitors cross the human placenta, and contrary to initially beliefs, may cause fetal cranial hypoplasia, anuria, reversible or irreversible renal failure, death, oligohydramnios, prematurity, IUGR, and PDA beginning with a 1st trimester exposure. There is no reason to expect perindopril is different.

Breastfeeding

There is no published experience in nursing women. It is unknown whether perindopril enters human breast milk.

Pregnancy

. Permethrin is rapidly metabolized to inactive metabolites that are excreted primarily in the urine. Although the amount of permethrin absorbed after a single application has not been precisely determined, preliminary study suggests it is less than 2% of the amount applied. There are no adequate reports or well-controlled studies in pregnant women. Permethrin improves maternal outcome when used as part of a broad strategy such as insecticide-incorporating nets.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether permethrin crosses the human placenta. However, recent large case series are reassuring. It is unlikely the maternal systemic concentration reaches a clinically relevant level. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Permethrin enters human breast milk, but the kinetics remain to be elucidated. Considering the route and frequency of use, it is unlikely a maternal clinically relevant systemic concentration will be reached and sustained.

Pregnancy

. Perphenazine is commonly combined with amitriptyline (Triavil, Etrafon) in the US. It increases circulating prolactin levels in both humans and rodents. There are no adequate reports or well-controlled studies in pregnant women. Some phenothiazines have been associated with a prolongation of the QT interval.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether perphenazine crosses the human placenta. However, peroxidative bioactivation of perphenazine by human placental peroxidase occurs and may be one mechanism of the reported toxicity of other phenothiazines. Postnatal behavioral abnormalities are suggested. Rodent teratogenicity studies apparently have not been conducted.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Perphenazine enters human breast milk. In one woman, the maternal levels were 2.1 and 3.2mcg/L after 16 and 24mg/d, and the M:P ratios were 1.1 and 0.7. The estimated dose to the infant ranged between 0.3 and 0.45mcg/kg/d, or <0.5% of the weight-adjusted maternal dose.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Mouse studies reveal synergy when phenacemide is administered with either mephenytoin, phenobarbital, or trimethadione.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether phenacemide crosses the human placenta. While it is difficult to separate the possible teratogenic effects from those of anticonvulsant agents used concurrently, limited rodent study suggests phenacemide is a teratogen.

Breastfeeding

There is no published experience in nursing women. It is unknown whether phenacemide enters human breast milk. 879

Pregnancy

. Phenazopyridine has a topical analgesic effect on urinary tract mucosa, helping to relieve pain, burning, urgency, and frequency. There are no adequate reports or well-controlled studies in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Phenazopyridine does not apparently cross the human placenta to any significant degree. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether phenazopyridine enters 880 human breast milk. However, it is generally considered compatible with Breastfeeding based on long clinical experience.

Pregnancy

. Phendimetrazine is a phenylalkylamine sympathomimetic with pharmacologic activity similar to amphetamine. Obese adult patients given dietary instruction and treated with ??anorectic?? drugs lost a fraction of a pound more during short-term trials compared to those treated with placebo and diet. Addiction is a risk. There is no published experience with phendimetrazine in pregnancy, and no indications for its use.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether phendimetrazine crosses the human placenta. Similar compounds do. Rodent teratogenicity studies have apparently not been performed. 881

Breastfeeding

There are no published studies in nursing women. It is unknown whether phendimetrazine enters human breast milk.

Pregnancy

. Depression is common during and after pregnancy, but typically goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. Phenelzine is often effective in treating depression characterized as atypical, nonendogenous, or neurotic. These patients frequently have anxiety and depression mixed with phobic or hypochondriacal features. There are no adequate reports or well-controlled studies of phenelzine in pregnant women. Most publications consist of case reports or small series. Many drugs interact with MAOIs. Well-documented and potentially fatal interactions between MAOIs and opioids, notably meperidine, require that labor analgesia be well planned in advance. Pressor agents should be avoided as even indirect- acting drugs can produce severe hypertension.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether phenelzine crosses the 882 human placenta. As for most psychotropic drugs, monotherapy and the smallest effective quantity given in divided doses may reduce risk by minimizing the systemic peaks. Rodent teratogenicity studies have apparently not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether phenelzine enters human breast milk.

Pregnancy

. Less time is spent in REM during barbiturate-induced sleep compared to normal sleep. Abrupt cessation may trigger increased dreaming, nightmares, and/or insomnia. Barbiturates provide little analgesia at subanesthetic doses; in fact, they may increase the reaction to painful stimuli. There are no adequate reports or well-controlled studies of phenobarbital in pregnant women. Several investigations indicate clearance is increased and 883 that periodic dose adjustment may be necessary. All adjustments should be guided by clinical symptoms. In addition, phenobarbital impacts the a number of liver CYPs. Phenobarbital is not effective for the treatment of cholestasis of pregnancy. Planned

Pregnancy

and counseling before conception are crucial. It is important to discuss folic acid supplementation, medication adherence, the risk of teratogenicity, and the importance of prenatal care.

Fetal Health

There are no adequate reports or well-controlled studies of phenobarbital in human fetuses. Barbiturates readily cross the human placental barrier and are distributed throughout fetal tissues, with highest concentration found in the placenta, fetal liver, and brain. The F:M ratio approximates unity. Withdrawal symptoms can occur in neonates exposed to barbiturates throughout the 3rd trimester. Case-control studies disagree on whether there is a relationship between barbiturate use and a higher than expected incidence of birth defects (oral clefting and cardiac malformations). Otherwise healthy women attempting suicide with barbiturates did not experience an increase in adverse

Pregnancy

outcomes. Antenatal phenobarbital exposure does not affect the neurodevelopmental outcome of preterm infants at 18-22mo of age. It also does not reduce the risk of neonatal IVH.

Breastfeeding

Phenobarbital enters human breast milk, and the magnitude is altered by polypharmacy especially early in breastfeeding. Breastfeeding is controversial because of the potential for slow elimination by some neonates. Infant sedation is possible, and the infant should be observed closely. Serum monitoring may be advisable if phenobarbital is continued during breastfeeding.

Pregnancy

. Phenoxybenzamine is a long-acting, a-receptor antagonist that creates a ??chemical sympathectomy.?? It increases blood flow to the skin, mucosa, and abdominal organs, and lowers both supine and erect BP. It has no effect on the parasympathetic system. There are no adequate reports or well-controlled studies in pregnant women. Though there are numerous case reports confirming its efficacy for pheochromocytoma during pregnancy, it does not reverse the acute decrease in maternal cardiac output associated with a hypertensive episode.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Phenoxybenzamine crosses the human placenta and is concentrated in the fetal plasma, achieving an F:M ratio of 3:1. Appropriate rodent studies apparently have not been conducted. 885

Breastfeeding

There is no published experience in nursing women. It is unknown whether phenoxybenzamine enters human breast milk.

Pregnancy

. Phensuximide suppresses the paroxysmal, 3cycles/sec spike-and- wave activity associated with the lapse of consciousness common in absence (petit mal) seizures. There is no published experience with phensuximide during pregnancy. Consideration may be given to stopping phensuximide if the severity and frequency of seizures are such they do not pose a serious threat to the patient. However, even minor seizures pose some hazard to the embryo and fetus.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether phensuximide crosses the human placenta. It is difficult to separate the impact of phensuximide from other agents used concurrently and the potential impact of 886 the seizures. The sole published estimate is that the risk is similar to ethosuximide. Limited rodent studies are reassuring.

Breastfeeding

There is no published experience in nursing women. It is unknown whether phensuximide enters human breast milk.

Pregnancy

. Phentermine is a sympathomimetic similar to amphetamine. It is indicated only for short-term monotherapy, and the associated weight loss is typically modest. Tachyphylaxis and tolerance occur with phentermine and all related drugs. Serious regurgitant disease of the aortic, mitral, and tricuspid valves occurs in patients taking a combination of phentermine and fenfluramine. The latter was withdrawn from the US market, but it is not definitive which drug was at fault. There are no adequate reports or well-controlled studies of phentermine in pregnant women, and there is probably no indication for its use during either

Pregnancy

or lactation. In one case-control study, the rate of gestational diabetes was significantly greater in the women who took phentermine and fenfluramine during the 1st trimester. In the guinea pig, mephentermine reduces uterine blood flow. Mephentermine appears as effective as ephedrine for the the treatment of hypotension associated with subarachnoid block.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether phentermine crosses the human placenta. Similar agents do cross. There was no significant increase in

Pregnancy

wastage or major malformations in almost 100 women who took phentermine and fenfluramine during pregnancy. Rodent teratogenicity studies have not been performed. A decrease in serotonergic axons in the hippocampus and mitral valve thickening was observed postnatally in pups of rats exposed to the combination antenatally.

Breastfeeding

There is no published experience in nursing women. It is unknown whether phentermine enters human breast milk.

Pregnancy

. Phentolamine is a short-acting a-antagonist with direct iono- and chronotropic actions. There are no adequate reports or well-controlled studies in pregnant women. There are a number of case reports documenting efficacy for the noted indications. Rodent studies suggest phentolamine reduces uterine contractility postpartum, but there is no clinical evidence of such activity in women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether phentolamine crosses the human placenta. Rodent studies are reassuring for the most part. Only in the mouse was there evidence of IUGR and skeletal delay after the maternal dose exceeded 25the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether phentolamine enters human breast milk.

Pregnancy

. Allergic rhinitis affects about1=3 of reproductive-age women. More than 170 OTC preparations contain a sympathomimetic agent as their active ingredient. Phenylephrine should be considered a second-line agent behind 1st- and 2nd-generation antihistamines. It is popular for the prevention of hypotension following neuraxial anesthesia during cesarean delivery especially when ephedrine might be contraindicated (e.g., maternal cardiac disease). There was no difference in the rostral spread of spinal hyperbaric bupivacaine with prophylactic phenylephrine than with ephedrine. However, there may be an unexplained increased incidence of fetal acidosis with ephedrine. Further, there is evidence that longer spinal-delivery intervals increased the risk of fetal acidosis developing with ephedrine, but not phenylephrine. No prophylactic technique seems to completely eliminate the need for treatment.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether phenylephrine crosses the human placenta. Pseudoephedrine is associated with intestinal atresias, but the same has yet to be reported for phenylephrine. The combination of pseudoephedrine, phenylephrine, and phenylpropanolamine (Triaminic) may be associated with distal limb reduction.

Breastfeeding

There is no published experience in Breastfeeding women. It is unknown whether phenylephrine enters human breast milk. However, considering the frequency of use, dose, and route, it seems unlikely the breastfed neonate would ingest a clinically relevant amount.

Pregnancy

. More than 170 OTC preparations contain a sympathomimetic agent as their active ingredient. An estimated 5 billion doses of phenylpropanolamine are taken each year. There are no adequate reports or well-controlled studies in pregnant women. The authors of one small RCT concluded that 50mg bid may be an effective and safe treatment in

Pregnancy

rhinitis. Ventricular arrhythmia during

Pregnancy

and intracranial hemorrhage postpartum are reported. The FDA required the removal of phenylpropanolamine in 2005 because of an increased risk of stroke. The agency estimated that it caused 200-500 strokes annually among 18-49y-old users.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether phenylpropanolamine crosses the human placenta. Epidemiologic studies are reassuring. Rodent reproduction and teratogenicity studies have not been conducted. Pseudoephedrine is associated with intestinal atresias, but similar data for phenylpropanolamine are not available. The combination of pseudoephedrine, phenylephrine, and phenylpropanolamine (Triaminic) is associated with distal limb reduction. Other epidemiologic evidence suggests a relationship between 1st trimester use and gastroschisis.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether phenylpropanolamine enters human breast milk.

Pregnancy

. Phenytoin is a 1st-generation, enzyme-inducing anticonvulsant. Stable phenytoin serum levels are achieved in most, though there is wide variability with equivalent doses. Patients with unusually low levels may be either noncompliant or hypermetabolizers. Unusually high levels can result from hepatic disease, congenital enzyme deficiency, or other drugs that interfere with metabolism. Clearance is increased during pregnancy, with concentrations declining to half of pre

Pregnancy

if the dose is not adjusted. Dose adjustments should be based on clinical symptoms, and not solely serum drug concentrations. Phenytoin is highly protein-bound, 892 and unbound drug levels are less affected than total concentrations. Phenytoin may impair the effect of corticosteroids, coumadin, digitoxin, doxycycline, estrogens, furosemide, oral contraceptives, quinidine, rifampin, theophylline, and vitamin D. Drug interactions between enzyme-inducing anticonvulsants such as phenytoin and contraceptives are well-documented. Either a higher dose oral contraceptive or a second contraceptive method is recommended. Planned

Pregnancy

and counseling before conception is crucial, and should include information on the risk of teratogenicity, need for folate supplementation, and the importance of prenatal care.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Phenytoin crosses the human placenta apparently by passive diffusion. The risk of major malformations in the offspring of women receiving AEDs is double the general population. Risk factors include dose and polytherapy. Phenytoin is specifically associated with congenital heart defects and cleft palate. There is evidence that a phenytoin-induced embryonic arrhythmia is one mechanism of teratogenicity. The arrhythmia reflects the ability of phenytoin to inhibit current in a specific potassium channel (IKr), and may cause embryonic ischemia-reperfusion injury with the generation of reactive oxygen species. Exposure to phenytoin in utero can lead to psychomotor delay. Either midface or digit hypoplasia correlates with neurodevelopmental compromise. In vitro, phenytoin causes neuronal cell death. Carbamazepine and topiramate alone did not induce neuronal death, but both drugs exacerbate phenytoin-induced cell death. In contrast, co-treatment with levetiracetam and carbamazepine does not enhance cell death in the developing brain. Thus, it may be possible to avoid proapoptotic effects, even in polytherapy, by choosing appropriate drugs. Prior reports of an increased risk of neonatal intracranial hemorrhage after in utero phenytoin exposure due to vitamin K deficiency have not been substantiated. As with most psychotropic drugs, the risks may be minimized by monotherapy and the smallest effective quantity given in divided doses to minimize the serum peaks.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. The transfer of phenytoin into human breast milk appears relatively low, and it is generally considered safe for breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of physostigmine in pregnant women. The published experience is confined to scattered case reports.

Fetal Health

There are no adequate reports or well-controlled studies of physostigmine in human fetuses. Considering the indications, dose, and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level unless the woman is being treated for anticholinergic syndrome.

Breastfeeding

There is no published experience in nursing women. It is unknown whether physostigmine enters human breast milk. However, considering the indication and dosing, physostigmine use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Hypoprothrombinemia may result from anticoagulation, antibiotic therapy, or GI disease, or may be drug-induced. The drugs listed are each vitamin K products with some pharmacologic differences. There are no adequate reports or well-controlled studies of phytonadione in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. While phytonadione crosses the human placenta, it varies with the compound and is limited, seeming to preclude a significant fetal effect. Placental transport is more efficient in the rat. Animal teratogenicity studies apparently have not been conducted. Phytonadione is often given to neonates in hopes of preventing IVH. The evidence for this practice is weak.

Breastfeeding

Phytonadione is concentrated in human breast milk, and may be useful as a supplement for the preterm, Breastfeeding neonate. It is generally considered compatible with breastfeeding.

Pregnancy

. There is no published experience with pilocarpine in pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pilocarpine crosses the human placenta. Only scant amounts cross the rat placenta (<.05%). In rabbits, pilocarpine accelerates fetal lung maturation.

Breastfeeding

There is no published experience during lactation. It is unknown whether pilocarpine enters human breast milk.

Pregnancy

. There is no published experience with pimecrolimus in pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pimecrolimus crosses the human placenta. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level. Rodent studies utilizing a topical application are reassuring, revealing no evidence of toxicity, teratogenicity, or IUGR despite the use of doses higher than those used clinically. Pimecrolimus does cross the rodent placenta after oral administration.

Breastfeeding

There are no published reports of pimecrolimus use during breastfeeding. It is unknown whether it enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of pimozide in pregnant women. The published literature is limited to a single case report where the outcome was normal. Pimozide produces a dose-dependent increase in pituitary tumors in rats.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether pimozide crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity, though IUGR and increased embryo resorption were noted at doses 8the MRHD.

Breastfeeding

There are no published reports of pimozide use in nursing women. It is unknown whether pimozide enters human breast milk. Pimozide stimulates prolactin secretion.

Pregnancy

. There is no recent published experience with iodoquinol during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether iodoquinol crosses the human placenta. Rodent teratogenicity studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether iodoquinol enters human breast milk.

Pregnancy

. Iohexol is a nonionic ragiographic contrast medium of low osmolality used extensively in clinical radiology. Side effects include transient malaise and vomiting.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Iohexol crosses the human placenta in significant concentration, and it was used to identify an omphalomesenteric duct cyst in a twin

Pregnancy

and a congenital diaphragmatic hernia in another. Breastfeeding There are no adequate reports or well-controlled studies in nursing women. Iohexol enters human breast milk, but <0.2% of the drug would be ingested by the unsupplemented neonate over 529 24h. These agents as a group are poorly absorbed orally (<1%), and the half-life of injected iohexol approximates 2h. As a result, iohexol seems to be of little risk to the

Pregnancy

. There is no published experience with ipecac during pregnancy. There is, however, a long clinical experience with its use to treat patients who have ingested toxic substances. Ipecac is cardiotoxic if not vomited.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown if ipecac crosses the human placenta. Rodent teratogenicity studies have not been performed. 530

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether ipecac enters human breast milk.

Pregnancy

. The published experience with ipratropium during

Pregnancy

is limited to case reports. Mild asthma during

Pregnancy

is managed with inhaled b2-agonists; therapy for moderate asthma includes inhaled cromolyn, inhaled beclomethasone, and oral theophylline. Severe gestational asthma should be treated with oral corticosteroids at the lowest effective dosage. The pharmacologic management of acute asthma during

Pregnancy

includes nebulized b2-agonists, ipratropium, and IV methylprednisolone.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether ipratropium crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. The highest doses (1000the MRHD) were associated with embryotoxicity. 531

Breastfeeding

There is no published experience in nursing women. It is unknown whether ipratropium enters human breast milk. While lipid-insoluble quaternary bases enter breast milk, it is unlikely ipratropium reaches the neonate to a significant degree since it is not well absorbed systemically after inhalation or oral administration.

Pregnancy

. The published experience with irbesartan during

Pregnancy

is limited to case reports and small series. Women taking inhibitors of renin-angiotensin should be placed on effective contraception and switched to another class of agents if they plan to or as soon as they become pregnant.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether irbesartan crosses the human placenta. Drugs that act directly on the renin-angiotensin system can cause perinatal morbidity and death. Adverse effects are noted in almost half of exposed pregnancies. Morbidity includes hypotension, neonatal skull hypoplasia, anuria, and reversible or irreversible renal failure. Oligohydramnios may be associated with limb contractures, craniofacial deformation, and hypoplastic lung development. Oligohydramnios may not appear 532 until after the fetus has sustained irreversible injury. Rarely, there is no alternative antihypertensive agent available. In these rare cases, women should be counseled on the hazards, and serial ultrasound examinations performed to assess the intra-amniotic environment. If oligohydramnios is observed, irbesartan should be discontinued unless lifesaving for the mother. Antenatal surveillance may be appropriate depending upon gestation.

Breastfeeding

There is no published experience in nursing women. While it is unknown whether irbesartan enters human breast milk, it is excreted at low concentration in rodent milk.

Pregnancy

. There is no published experience with irinotecan during pregnancy. Women of childbearing potential should be advised to avoid becoming pregnant while receiving irinotecan.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether irinotecan crosses the human placenta, but it does cross the rat placenta. Rodent teratogen studies reveal irinotecan is embryotoxic and teratogenic, causing a variety of external, visceral, and skeletal abnormalities, along with decreased learning. 533

Breastfeeding

There is no published experience in nursing women. It is unknown whether irinotecan enters human breast milk. Irinotecan is concentrated in rodent breast milk, and should probably be considered incompatible with Breastfeeding until further study.

Pregnancy

. There is no evidence that iron supplementation improves

Pregnancy

outcome in the industrialized world. That is not true, however, in developing countries where the treatment of iron deficiency anemia reduces both the antenatal and postnatal maternal morbidity and mortality. Under these circumstances, iron dextran is more effective than oral treatment in correcting anemia and reducing the need for transfusion. The IM administration of 3 doses (250mg Fe) at monthly intervals appears effective and well tolerated; it may be used in women who cannot tolerate oral iron. However, IM administration of iron is appropriate only in hospital settings well equipped to treat an anaphylactic crises. Folic acid supplementation is recommended.

Fetal Health

There are no adequate reports or well-controlled studies of iron dextran in human fetuses. Iron crosses the placenta, but the effect of supplementation on that transport is unclear. There is some evidence that maternal iron dextran IV supplementation increases the fetal iron stores, but it is unclear which form of iron crosses.

Breastfeeding

Maternal iron supplementation does not alter the concentration of iron in breast milk, though traces of unmetabolized iron dextran are found in human milk.

Pregnancy

. Depression is common during and after pregnancy, but typically goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. A major depressive episode (DSM-IV) implies a prominent and relatively persistent (almost every day for at least 2w) depressed or dysphoric mood that interferes with daily functioning. It includes at least 5 of the following 9 symptoms: depressed mood, loss of interest in usual activities, significant change in weight and/or appetite, insomnia or hypersomnia, psychomotor agitation or retardation, increased fatigue, feelings of guilt or worthlessness, slowed thinking or impaired concentration, and a suicide attempt or suicidal ideation. There are no adequate reports or well-controlled studies of isocarboxazid in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether isocarboxazid crosses the human placenta; it does cross the rat placenta. Rodent teratogenicity studies have not been performed. Prolonged treatment during rodent

Pregnancy

is associated with behavioral changes.

Breastfeeding

There is no published experience in nursing women. It is unknown whether isocarboxazid enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Isoflurane has been used clinically without pregnancy-related sequelae for many years. Like other halogenated anesthetic agents, isoflurane produces uterine relaxation. The inhibitory potency of sevoflurane and desflurane are comparable to, whereas that of isoflurane is smaller than, halothane. Minimum alveolar concentrations causing a 50% inhibition of the contractile amplitude were 1.7, 1.4, 2.35, and 1.7 (p <.05), respectively.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Isoflurane rapidly crosses the human placenta, achieving an F:M ratio approximating unity. It has been used for fetal surgery and to facilitate uterine maneuvers. Isoflurane produces moderate fetal hypotension and bradycardia in sheep. However, fetal cerbral oxygenation remains constant despite a decrease in the fetal MAP by 20%. More recently, evidence has emerged that at least in rodents, exposure to such agents leads to neuroapoptosis with permanent brain damage. 537

Breastfeeding

There is no published experience in nursing women. It is unknown whether isoflurane enters human breast milk. However, considering the indications and dosing, one-time isoflurane use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Isoniazid is metabolized primarily by acetylation and dehydrazination. Approximately half of blacks and Caucasians are ??slow acetylators?? and the rest ??rapid acetylators??; the majority of Eskimos and Orientals are rapid acetylators. The rate of acetylation does not significantly alter effectiveness, but slow acetylation may lead to higher blood levels and increase toxicity. The risk of isoniazid-induced hepatitis is age-related and 538 increased by alcohol ingestion. TB is experiencing a ??rebirth?? in many countries, and untreated TB in

Pregnancy

is a significant threat to mother, fetus, and family. Women with untreated HIV and TB are at particular risk of death. Pregnant women in the US but born in another country should be screened for TB at the first prenatal visit. There are no adequate reports or well- controlled studies of isoniazid in pregnant women. Adherence to treatment is especially difficult because of a general fear of any medication and pregnancy-related nausea. All 4 first-line drugs (isoniazid, rifampin, ethambutol, and pyrazinamide) have an excellent safety record in pregnancy. Prophylactic pyridoxine is indicated. Antepartum treatment of latent TB has the greatest likelihood of success secondary to a higher degree of compliance.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Isoniazid crosses the human placenta, but has not been associated with an increased risk of malformations. Congenital TB is rare but does occur. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity may occur in some rodents.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only scant amounts of isoniazid are excreted into human breast milk. It is generally considered compatible with breastfeeding, and is not adequate treatment for neonatal TB. In addition to isoniazid, rifampin, ethambutol, and streptomycin (first-line agents), as well as kanamycin and cycloserine (second-line agents), are considered by the American Academy of Pediatrics to be compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of isoproterenol in pregnant women. It has been suggested its addition to epidural bupivacaine and sufentanil speeds the onset of analgesia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Isoproterenol crosses the human placenta, though the kinetics remain to be elucidated. It has been used (unsuccessfully) to treat fetal complete CHB. There are no reports of fetal compromise associated with isoproterenol despite numerous case reports and series. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether isoproterenol enters human breast milk. Other b-agonists are considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Isosorbide dinitrate may be a useful alternative treatment for acute hypertension in women with severe preeclampsia (5mg SL). In one small study of preeclamptic women, sustained use was associated with a decline in the uterine artery Doppler-measured flow resistance. It was used in one instance to facilitate the manual removal of a retained placenta.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether isosorbide dinitrate crosses the placenta. SL administration has no effect on the FHR pattern. In one small study of preeclamptic women, sustained use was associated with a decline in the umbilical artery Doppler- measured flow resistance and the maximum AF pocket increased. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity occurs in rodents with doses 50- 100the MRHD.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether isosorbide dinitrate enters human breast milk.

Pregnancy

. There are several case reports of its use in pregnant women with an acute MI. Isosorbide mononitrate is absorbed across the vaginal mucosa. It was investigated as a cervical ripening agent prior to 1st trimester abortion. It has also been studied as a cervical ripening agent where it (20 or 40mg) increases the maternal pulse rate and the maternal systolic and pulse pressures. In another RCT comparing it to misoprostol, misoprostol was superior for cervical ripening though both drugs were associated with a high frequency of Side effects include orthostatic hypotension, palpitations, arrhythmia, chest pain, thrombocytopenia, N/V, headache, blurred vision, asthenia, dry mouth, constipation, abdominal pain, flatulence, bronchitis, sinusitis, and rash.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. In the studies of its use either as a cervical ripening agent or treatment for preeclampsia, isosorbide mononitrate produced Doppler changes consistent with a maternal systemic effect. In another study where cervical ripening 543 was the indication, isosorbide mononitrate (40mg) increased the FHR some 15 bpm. There was no significant effect on umbilical artery resistance. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity occurs in rodents with doses 50-100the MRHD. Breastfeeding There are no adequate reports or well-controlled studies in nursing women. It is unknown whether isosorbide mononitrate enters human breast milk.

Pregnancy

. Isotretinoin is contraindicated during pregnancy. Only manufacturer-approved physicians may prescribe it. Though many fail to comply patients must be capable of complying with mandatory contraceptive measures. Patients should be cautioned not to self-medicate with St. John?s wort because of a possible interaction with oral contraceptives, increasing the risk of an unplanned pregnancy. It is critical women of childbearing potential select and commit to use 2 forms of effective contraception simultaneously, at least 1 of which must be a primary form, unless absolute abstinence is the chosen method, or the patient has undergone a hysterectomy. In one study, a cohort of 8609 women between 13 and 45 years of age with a first prescription for isotretinoin was identified. Pregnancies, spontaneous and elective abortions, and birth defects were identified using procedure codes and medical diagnoses. Ninety (90) became pregnant for an annual

Pregnancy

rate of 32.7/1000 person-years of treatment. Of these, 76 terminated, 3 had a spontaneous abortion, and 2 had trauma during delivery resulting in neonatal death. There were only 9 live births. Among the live births, only one had a congenital anomaly of the face and neck (11%). Adjusting for potential confounders, predictors of becoming pregnant while on isotretinoin were lower socioeconomic level, one or more visits to the doctor or to the emergency department, or one or more hospitalization while on isotretinoin; concomitant isotretinoin and oral contraceptive use had a preventive effect.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Isotretinoin and its active metabolites crosses the human (and subhuman primate) placenta, and it is a known human teratogen. Multiple organ systems are affected, including CNS, CV, and endocrine organs. Mental retardation without external malformation has also been reported. Similar malformations occur in rodents.

Breastfeeding

There is no published experience in nursing women. It is unknown whether isotretinoin enters human breast milk. Considering its effect on the fetus, Breastfeeding is considered contraindicated.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Calcium channel antagonists may be the tocolytic of choice based on their performance in meta-analyses. In vitro, isradipine is a superior tocolytic compared to ritodrine and magnesium sulfate. It has been used with success to treat preeclamptic hypertension with efficacy similar to methyldopa prior to delivery.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. While isradipine crosses the human placenta, achieving an F:M ratio of about 0.25, Doppler-measured resistances in the umbilical artery are unaltered. Rodent studies are reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. There is, however, an increased frequency of IUGR at the highest doses studied.

Breastfeeding

There is no published experience in nursing women. It is unknown whether isradipine enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of itraconazole in pregnant women. There are several case reports of its use during

Pregnancy

without note of diminished efficacy. There are also reports suggesting that the efficacy of oral contraceptives to block ovulation may be reduced by simultaneous use of itraconazole.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Itraconazole interacts with a major placental transporter, P-glycoprotein. In one prospective cohort study, there was no evidence of teratogenicity or fetal sequelae. In rodents, doses of itraconazole 5-20the MRHD were associated with maternal and embryotoxicity, and teratogenicity in the survivors, consisting predominantly of skeletal defects. In another rodent study, skeletal defects occurred after early exposure (day 8), while cleft lip and palate were seen following later exposure (day 13).

Breastfeeding

There is no published experience in nursing women. Itraconazole enters human breast milk, but the pharmacokinetics are presently unclear. According to the manufacturer, the maximum M:P ratio is 1.77, the milk concentration is 70mcg/L, and a theoretic infant dose is 10mcg/kg/d.

Pregnancy

. There are no adequate reports or well-controlled studies of ivermectin in pregnant women. The few published cases report no sequelae. Further, there have been several mass exposures of pregnant women during community-based treatment of onchocerciasis. No increase in adverse

Pregnancy

outcomes was noted.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is not known whether ivermectin crosses the 549 human placenta; it does appear to block P-glycoprotein?mediated efflux. There have been several mass exposures of pregnant women during community-based treatment of onchocerciasis. No increase in

Pregnancy

wastage or malformations was observed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only1=3 of the maternal plasma ivermectin level is achieved in human breast milk. It is unlikely to pose a clinically significant risk to the Breastfeeding infant.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Kanamycin is a second-line agent for the treatment of TB, but is otherwise not used widely during

Pregnancy

and offers no advantages over other aminoglycosides. Routine monitoring of peak and trough levels is not required in otherwise healthy women with normal renal function.

Fetal Health

There are no well-controlled studies in human fetuses. Case reports suggest the degree of human placental transfer is incomplete. Kanamycin crosses the placenta in rodents, and most likely in humans, as other aminoglycosides do. There is no evidence of teratogenicity for any of the aminoglycosides. In guinea pigs, doses of kanamycin 20the MRHD had no obvious Side effects . However, otic nerve damage has been reported after an in utero?exposed neonate was challenged postnatally. Breastfeeding There are no adequate reports or well-controlled studies in nursing women. Kanamycin enters human breast milk, but is generally considered compatible with breastfeeding.

Pregnancy

. Ketamine is a rapid-acting general anesthetic agent. There are no adequate reports or well-controlled studies in pregnant women. It is popular in some locales for cesarean delivery of parturients who are either hemorrhaging or have asthma (increased catecholamine release ameliorates bronchospasm) or fetal acidemia. Compared to thiopental, women who receive ketamine during cesarean delivery have a lower need for supplemental analgesia postoperatively. The incidence of awareness to verbal commands during surgery is lower with ketamine compared to thiopental, but the frequency of recall of intraoperative events is not different. There is reportedly an increased incidence of dreaming during anesthesia, which may lead to dissatisfaction with the anesthetic experience. Ketamine has also been used with neuraxial anesthesia. In women undergoing cesarean section with spinal analgesia, the addition of ketamine (0.05mg/kg) intrathecally to 10mg of spinal plain bupivacaine (0.5%) led to rapid onset of both sensory and motor blockade and enhanced the segmental spread of spinal block without prolonging the duration of analgesia, while fentanyl provided prolonged analgesia. In other studies, IV low-dose ketamine combined with intrathecal bupivacaine was reported to provide longer analgesia after cesarean section and lower postoperative analgesic consumption than bupivacaine alone, suggesting a preemptive effect.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. A number of rodent studies suggest ketamine may alter postnatal behavior and taste appreciation with early exposure. In sheep, ketamine attenuates hemodynamic responses to cerebral hypoperfusion and is a potent inhibitor of ACTH and pro-opiomelanocortin/pro-ACTH release.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether ketamine enters human breast milk. However, considering its application, it is unlikely a clinically significant amount of drug would remain in breast milk at least 48h postoperatively.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Ketoconazole is a known aromatase inhibitor and may alter sex hormone levels. Although the drug is absorbed when applied topically, the systemic concentration is relatively low. Ketoconazole has been used to treat Cushing?s syndrome during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Ketoconazole is a P-glycoprotein substrate, though placental transfer has not apparently been studied. Several studies suggest ketoconazole interferes with ovarian synthesis of progesterone by inhibiting aromatase. As such, it could interfere with implantation and maintenance of early pregnancy. However, limited epidemiological studies are reassuring. Ketoconazole produced maternal toxicity along with syndactyly and oligodactyly in rodents exposed to 10the MRHD.

Breastfeeding

Only a trace amount of maternally administered ketoconazole enters human breast milk, and it is generally considered safe during breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Ketoprofen provides effective analgesia after both vaginal and cesarean delivery, but its efficacy is similar to other NSAIDs such as diclofenac.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Ketoprofen rapidly crosses the placenta, reaching an F:M ratio approaching unity. Most other NSAIDs can produce fetal oliguria and ductal constriction in a dose- and gestational age?dependent fashion. One case report suggests ketoprofen has the same actions. Another study suggests the active S isomer is preferentially transported across the term placenta. Further, acute renal failure is reported in preterm infants whose mothers received ketoprofen prior to delivery. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR.

Breastfeeding

Low concentrations of ketoprofen are found in human breast milk, but the breastfed infant would consume less than 1% of the maternal weight adjusted dose.

Pregnancy

. Ketorolac is indicated for the management of pain that usually would require an opioid for relief. There are no adequate reports or well-controlled studies in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether ketorolac crosses the placenta. Most other NSAIDs can produce fetal oliguria and ductal constriction in a dose- and gestational age?dependent fashion. It is not known whether ketorolac has the same actions. 557 Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR. The perinatal mortality rate in rodents was increased in association with delayed onset of parturition.

Breastfeeding

Small quantities of ketorolac enter human breast milk. An unsupplemented newborn would ingest <0.4% of the daily maternal dose.

Pregnancy

. Hypertensive disorders complicate 5-10% of pregnancies and are a leading cause of maternal and perinatal morbidity and death. Severe hypertension (systolic BP >170mmHg and/or diastolic BP >110mmHg) should be treated rapidly to reduce the risk of stroke, death, and possibly eclampsia in preeclamptic women. There is no consensus whether mild to moderate hypertension should be treated during pregnancy. The risks of transient severe hypertension, the likelihood of antenatal hospitalization, proteinuria at delivery, and neonatal RDS may be decreased by therapy. Labetalol reduces BP more slowly than nifedipine, and it does not increase the maternal cardiac index as nifedipine does. Thus, labetalol is the drug of choice for hypertensive women with tachycardia. Labetalol has a lower risk of hypotension than parenteral hydralazine. Labetalol is better tolerated than methyldopa and provides more efficient BP control. It reduces cerebral pressure without altering cerebral perfusion. IV labetalol is equally effective as IV hydralazine for the treatment of postpartum hypertension. Labetalol may also be useful for the treatment of maternal thyrotoxicosis during labor.

Fetal Health

Labetalol crosses the human placenta, yielding an F:M ratio of 0.5 and an AF:M ratio <0.20. Neither labetalol nor hydralazine vasodilates the perfused human cotyledon. Doppler flow studies reveal no change in umbilical, uterine, and middle cerebral resistances after treatment. IV labetalol can cause fetal bradycardia. The available data are inadequate to determine whether labetalol adversely affects fetal or neonatal HR and pattern. Until such data are available, FHR changes should not be attributed to a drug effect, but rather to progression of the underlying maternal or placental disease. Hypoglycemia, bradycardia, hypotension, pericardial effusion, and myocardial 559 hypertrophy are reported after long-term oral labetalol. Fetal death may also occur after a sudden drop in the maternal BP, the risk of which can be minimized by adequate hydration. Overall, neonatal outcome is similar to that achieved with hydralazine. Labetalol may be useful for the treatment of fetal thyrotoxicosis. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Labetalol reduces uteroplacental blood flow selectively in guinea pigs, perhaps explaining the increased frequency of IUGR in this model.

Breastfeeding

There is no consistent relation between maternal plasma and milk concentrations either within or between individuals. The risk of hypoglycemia in breastfed neonates is increased by labetalol but may be blunted with glucose-fortified formula.

Pregnancy

. Constipation is common during pregnancy. Lactulose helps restore normal bowel habits. It is poorly absorbed, and women with lactose intolerance tolerate lactulose better in the 3rd trimester because of slow transit and bacterial adaptation. It is 561 used by some to maintain a soft stool after delivery complicated by rectal extension.

Fetal Health

There are no adequate reports or well-controlled studies of lactulose in human fetuses. Because of poor maternal absorption, it is unlikely the maternal systemic concentration will reach a clinically relevant level. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether lactulose enters human breast milk. Because of poor maternal absorption, it is unlikely the maternal systemic concentration will reach a clinically relevant level. Breastfeeding infants require lactase to metabolize lactose, the major carbohydrate in breast milk. Lactase is located on the small intestinal brush border and is extremely vulnerable to pathogenic damage.

Pregnancy

. There are no adequate reports or well-controlled studies of lamivudine in pregnant women. Lamivudine is rapidly absorbed after oral administration, reaching maximal serum concentrations after 30-90min. Triple therapy (zidovudine, lamivudine, nevirapine) is a highly effective regimen. However, there are reports of rapid development of genotypic resistance to lamivudine. HIV therapy that reduces the viral load significantly reduces the risk of mother-to-child transmission. Hepatotoxicity, usually within 5mo of beginning therapy, is a major concern during pregnancy. It is most severe when associated with HBV and HCV co-infection. There are presently only 2 drugs for the treatment of hepatitis B during pregnancy?interferon alfa-2b and lamivudine. The initial response to lamivudine is superior to interferon alfa-2b. Lamivudine is reportedly safe in pregnant women with chronic HBV infection during the last weeks of pregnancy. However, reduced HBV particle number does not necessarily translate into decreased vertical transmission. Further, resistant HBV strains develop in some patients. US federal government guidelines recommend zidovudine plus lamivudine for health care personnel exposed to both HBV and HIV.

Fetal Health

The worldwide spread of HIV-1 has resulted in an estimated 1 million children born yearly to HIV-1?infected mothers. In the absence of antiretroviral intervention, about 25% are HIV-1 infected. Maternal AZT prophylaxis reduces the rate of neonatal transmission to some 7%, with further reductions with combination therapy including lamivudine. Lamivudine readily crosses the human placenta; the AF:M ratio reportedly varies from unity to 4. This level does not necessarily prevent HBV transmission to the perinate despite undetectable maternal viral DNA. Large trials are awaited. Relative and absolute polymerase chain reaction quantification reveals a 3- to 4-fold mean increase in MDR1 placental transcription in HIV-infected women. Further, there is a 2.5-fold increase of immunoreactive P-glycoprotein in placentas from HIV-infected women. This MDR1 overexpression is observed regardless of antiretroviral therapy. This suggests that P-glycoprotein in placentas from 563 HIV-infected women would modulate the maternofetal transport of antiretrovirals across the placental barrier and consequently decrease fetal exposure to these compounds. Neonatal prophylaxis with both zidovudine and lamivudine is typically initiated within 12h of birth. Mitochondrial disorders are described in children exposed in utero to some reverse transcriptase enzyme inhibitors (e.g., zidovudine). While rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically, embryotoxicity occurs in rabbits. In monkeys, lamivudine becomes incorporated into the DNA of multiple fetal organs and telomere shortening occurs. In human infants, lamivudine incorporation as well as HPRT and glycophorin A assay (GPA) mutagenesis have been documented in cord blood from infants exposed in utero to zidovudine and lamivudine. Given the risk:benefit ratio, these highly successful drugs will continue to be used for prevention of vertical viral transmission; however, evidence of genotoxicity suggests exposed children should be followed well past adolescence for early detection of potential cancer hazard.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Lamivudine is excreted into human breast milk, though the kinetics remain to be elucidated. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission. However, in women receiving zidovudine, lamivudine, and nevirapine (HAART) from 28w of gestation to 1mo postpartum, median M:P ratios were 1.1, 0.6, and 1.8, respectively. HIV RNA levels in breast milk were significantly lower than in untreated women (median of 2.3 vs. 3.4 log at delivery and 1.9 vs. 3.6 log at day 7; p <.001 for both comparisons). Almost 90% of treated women have less than 50 copies/ml compared to only1=3 of untreated women. DNA loads are unaffected. Thus, antiretroviral a

Pregnancy

. Most pregnancies are uneventful in women with epilepsy, and most babies are delivered healthy with no increased risk of obstetric complications in women. There are no adequate reports 565 or well-controlled studies of lamotrigine during pregnancy. Concerns over teratogenicity of AEDs must be weighed against the risks to the mother and fetus of seizures. Therapeutic drug monitoring has therefore been recommended to control for changes in the disposition of the older generation AEDs during pregnancy. Much less is known about gestation-induced alterations in the pharmacokinetics of the AEDs that have been introduced in the last 15y. Lamotrigine is by far the most extensively studied of the newer AEDs. Lamotrigine clearance is increased during pregnancy, and many women require a higher dose to maintain therapeutic levels. Pronounced alterations have been reported, with an increase of >300% from baseline in late

Pregnancy

in some patients on monotherapy. The available data suggest the associated decline in plasma concentrations is associated with loss of seizure control. Limited data indicate a similar decline in late

Pregnancy

in plasma concentrations of the active monohydroxy derivative of oxcarbazepine. Adjustments are based on clinical symptoms, not solely on serum drug levels. Lamotrigine is an inhibitor of dihydrofolate reductase. Adequate folate supplementation beginning preconception is wise. The impact of

Pregnancy

on clearance reverses quickly postpartum. The most frequent adverse maternal effect is skin rash, typically in the first month of treatment. Planned

Pregnancy

and counseling before conception is crucial. Counseling should cover folate supplementation, the importance medication compliance, the risk of teratogenicity, and the importance of prenatal care. Lamotrigine increases the metabolism of ethinyl estradiol and progestogens; a preparation containing at least 50mcg of ethinyl estradiol is recommended.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Lamotrigine crosses the human placenta, achieving an F:M ratio near unity. Women taking anticonvulsant medication of any type have a 4-8% risk of delivering a child with a birth defect compared to 2-4% in the general population. Lamotrigine inhibits dihydrofolate reductase, an enzyme necessary for the biosynthesis of nucleic acids and proteins. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR at doses analogous to human. The highest doses cause maternal and fetal toxicity characterized by IUGR and ventricular dilation. Though some data are conflicting, registry data do not reveal a significant increase in the risk of major malformation (2.8% for 1st trimester exposure with monotherapy, but 4.3% with polytherapy). Use of monotherapy at the lowest effective quantity given in divided doses to minimize the peaks can minimize the risks. Recent

Pregnancy

databases suggest valproate is significantly more teratogenic than carbamazepine, and the combination of valproate and lamotrigine is particularly teratogenic.

Breastfeeding

The median M:P ratio ranges from 0.5 to 0.8 2-3w postpartum, and nursed infants maintain plasma concentrations approximating 30% of the mother?s plasma level. While no adverse effects have been reported, the infant should be monitored closely if the mother elects to breastfeed, the drug given at the lowest effective dose, and Breastfeeding avoided at times of peak drug levels. 566

Pregnancy

. GERD and/or heartburn occur in 45-85% of women during pregnancy. The effect of estrogen and progesterone on lower esophageal sphincter tone is a recognized factor. The treatment of GERD consists of reducing gastric acidity following a step-up algorithm beginning with lifestyle modifications and dietary changes. Antacids or sucralfate are first-line medical therapy, 568 followed by histamine receptor antagonists. Ranitidine is probably preferred because of its documented efficacy and safety profile in pregnancy, even in the 1st trimester. Proton pump inhibitors are reserved for the woman with intractable symptoms or complicated reflux disease. However, proton pump inhibitors such as lansoprazole are generally considered effective treatment for GERD in pregnant women, and the findings of a recent prospective multicenter trial are reassuring. Adverse effects have not been reported. Further, proton pump inhibitors are first-line agents for the prevention of ??aspiration syndrome?? during general anesthesia. Lansoprazole has also been used with apparent success to treat a woman with Zollinger Ellison syndrome during pregnancy.

Fetal Health

There are no well-controlled studies in human fetuses. It is unknown whether lansoprazole crosses the human placenta. Epidemiologic and post-marketing surveillance studies are reassuring. Rodent studies too are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether lansoprazole enters human breast milk. It is excreted into rodent milk.

Pregnancy

. The published experience with latanoprost during

Pregnancy

is limited to case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether latanoprost crosses the human placenta. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level. Embryotoxicity was observed in rodents treated with a dosage more than 15the MRHD.

Breastfeeding

There is no published experience in pregnancy. It is unknown whether latanoprost enters human breast milk. However, considering the dose and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. The published literature during

Pregnancy

is limited to case reports of 1st/2nd trimester exposures. Based on animal study (see Fetal Considerations), leflunomide is contraindicated during

Pregnancy

and effective contraception is a must. Women desiring

Pregnancy

must discontinue leflunomide before conceiving, preferably at least 4mo before. Further, the manufacturer recommends preconception treatment with cholestyramine to increase drug elimination with subsequent verification that plasma levels are less than 0.02mg/L.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Leflunomide likely crosses the human placenta. No pattern of malformations has been reported in infants exposed to leflunomide, but the number of reported

Pregnancy

outcomes is small. In an ongoing prospective controlled study of rheumatoid arthritis (RA) medications in

Pregnancy

being conducted by OTIS, 43 leflunomide-exposed women were compared to 78 women with RA who did not use leflunomide and with a second group of 47 women without RA. Preliminary data indicate rates of major birth defects were similar in all 3 groups. Infants exposed to leflunomide were significantly more likely than infants of women without RA to be born prematurely and to be smaller. There were, however, no significant differences in these 2 measures between leflunomide-exposed infants and nonexposed infants of women with RA, suggesting that the underlying disease or other medications used to treat RA are likely associated with these adverse outcomes. The incidences of anophthalmia and micropthalmia are increased in rats treated with only 0.1the concentration recommended in humans. In rabbits, a dose analogous to the human is associated with embryotoxicity and bony abnormalities.

Breastfeeding

There is no published experience in nursing women. It is unknown whether leflunomide enters human breast milk. In light of the animal studies, it is best to avoid Breastfeeding if leflunomide must be prescribed. 571

Pregnancy

. Heparin-induced thrombocytopenia is a rare but potentially life- threatening reaction to both heparin and LMWH. It is the most common drug-induced immune-mediated thrombocytopenia. Lepirudin effectively treats the thrombocytopenia by inhibiting thrombin. Many patients develop antibodies (40%), and the aPTT should be monitored during long-term therapy. The published experience during

Pregnancy

is limited to a few case reports, including 1st trimester treatment.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether lepirudin crosses the human placenta; it does cross the rat placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether lepirudin enters human breast milk.

Pregnancy

. Letrozole is a nonsteroidal aromatase inhibitor that significantly lowers estradiol and estrone. It is used mostly for adjuvant therapy. Letrozole has also been used to treat infertility associated with poor response to FSH stimulation. There is no published experience during pregnancy.

Fetal Health

There are no well-controlled studies in human fetuses. It is unknown whether letrozole crosses the human placenta. The scant human study is reassuring. There is no difference in the overall rates of major and minor congenital malformations among newborns of women who conceived after letrozole or clomiphene treatments. However, it appears that congenital cardiac anomaly is less frequent in the letrozole group. Letrozole is embryotoxic, fetotoxic, and teratogenic in rodents even at low doses. Since in the primate estrogen modulates placental vascular endothelial growth/permeability factor expression and angiogenesis, letrozole could conceptually impact placentation.

Breastfeeding

There is no published experience in nursing women. It is unknown whether letrozole enters human breast milk.

Pregnancy

. Gestational trophoblastic disease is a spectrum of disorders ranging from the benign complete or partial hydatidiform mole to malignant choriocarcinoma. While the preponderance of women are cured by surgery, the occasional patient requires chemotherapy. Methotrexate, an inhibitor of dihydrofolate reductase, is the first-line agent. It can persist in human tissue for long periods. Leucovorin is a derivative of tetrahydrofolate and as such circumvents the block. Supplementation minimizes toxicity and can counteract inadvertent overdose. Methotrexate may be given as a single dose IM, which usually does not require leucovorin, or in a multiple-dose regimen, which does require leucovorin rescue. Methotrexate with leucovorin rescue is a highly effective, well-tolerated, nonsurgical treatment for patients with ectopic pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses (see folic acid). Folate is quickly transferred across the placenta. Rodent teratogenicity studies have not been conducted. Periconceptional folate supplementation increases fertility (higher cumulative rates and of multiple births). A deficiency of folic acid increases the incidence of NTDs, and randomized studies reveal that 4mg/d of folic acid prior to conception prevents their recurrence. It is not known whether leucovorin supplementation would have the same effect.

Breastfeeding

There is no published experience in nursing women. It is unknown whether leucovorin enters human breast milk.

Pregnancy

. Gonadotropin-releasing agonists are important for the treatment of infertility and are often used with IVF. There are no adequate reports or well-controlled studies of leuprolide during pregnancy, nor is there an indication for its use.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether leuprolide crosses the human placenta. No malformations are reported in women inadvertently exposed to leuprolide during pregnancy. 576 However, early exposure of a male fetus may lead to micropenis. Rodent studies reveal a dose-dependent increase in the incidence of major malformations and IUGR.

Breastfeeding

There is no published experience in nursing women. It is unknown whether leuprolide enters human breast milk.

Pregnancy

. Levalbuterol is at least as effective as other b2-adrenergic agonists for the treatment or prevention of bronchospasm. There is no published experience with levalbuterol during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether levalbuterol crosses the human placenta. Maternal systemic plasma levels are low after inhalation. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. In contrast, other b2-adrenergic agonists (e.g., albuterol, isoproterenol) have been associated with cleft palate and NTDs.

Breastfeeding

There is no published experience in nursing women. It is unknown whether levalbuterol enters human breast milk. However, considering the indication and dosing, occasional levalbuterol use is unlikely to pose a clinically significant risk to the Breastfeeding neonate. 577

Pregnancy

. Levamisole is an immunomodulator often used as adjuvant treatment for colon cancer. It is also used as an antirheumatic and anthelmintic drug. There is limited use in pregnancy, mostly as a deworming agent in developing countries. One post- marketing report is reassuring. 578

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether levamisole crosses the human placenta. One post-marketing report is reassuring. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity was noted in some studies.

Breastfeeding

There is no published experience in nursing women. It is unknown whether levamisole enters human breast milk. Levamisole is excreted into cow?s milk and reportedly stimulates production.

Pregnancy

. Levetiracetam is unrelated to other AEDs, and is used for the treatment for partial-onset seizures. Case series suggest it is well- tolerated during pregnancy. Maternal clearance increases such that 3rd trimester levels are only 40%-50% of baseline absent a dose adjustment. Those women who become or who are planning to become pregnant while taking levetiracetam should supplement their folic acid intake. Once pregnant, dosage 579 readjustments may be necessary and should be based on clinical symptoms, and not exclusively on serum drug concentrations. A specific drug registry for women exposed to levetiracetam during

Pregnancy

has been established by the manufacturer (1-888-537-7734).

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. In one series of 11 exposed pregnancies, there were 3 neonates with IUGR. Levetiracetam crosses the human placenta, achieving an F:M ratio of 0.56-2.0. In vitro, carbamazepine and topiramate alone did not induce neuronal death; both drugs exacerbate phenytoin-induced cell death. In contrast, co-treatment with levetiracetam and carbamazepine did not enhance cell death in the developing brain. Thus, it may be possible to avoid proapoptotic effects, even in polytherapy, by choosing appropriate drugs. Levetiracetam, as monotherapy or in combination, may be a promising candidate for the treatment of women during

Pregnancy

and for preterm and neonatal infants. Rodent studies conducted using doses in excess of the MRHD reveal embryotoxicity and an increased prevalence of skeletal malformations.

Breastfeeding

Levetiracetam enters human breast milk. In two small studies of 11 women, the mean M:P ratio approximated 1. The calculated neonatal dose was estimated to be 2.4mg/kg/d, equivalent to 8.0% of the weight-normalized maternal dose. Plasma concentrations in breastfed newborns were approximately 13% of the mother?s level.

Pregnancy

. There is no published experience with levocabastine during pregnancy. Approximately1=3 of childbearing-age women have allergic rhinitis. Immunotherapy, cromolyn, and beclomethasone are first-line agents because of their safety record.

Fetal Health

There are no adequate reports or well-controlled studies of levocabastine in human fetuses. Considering the dose and route, it is unlikely the maternal systemic concentration reaches a clinically relevant level. In rodents, levocabastine caused polydactyly at doses 16,500the ocular MRHD; polydactyly, hydrocephaly, brachygnathia, and embryo and maternal toxicities occur at doses 66,000the ocular MRHD.

Breastfeeding

There is no published experience with levocabastine in nursing women. The manufacturer?s reports suggest a trace amount is excreted. However, considering the dose and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. Parkinson?s disease is characterized by neuronal degeneration in the corpora nigra. Evidence suggests the symptoms are related to depletion of striatal dopamine. Parkinson?s disease manifests before age 40y in about 5% of patients. Limited experience suggests symptoms often worsen during pregnancy, and may not return to baseline postpartum. Levodopa is the first-line agent and is usually combined with carbidopa. There are no adequate reports or well-controlled studies of levodopa in pregnant women. Several case reports describe successful outcomes without obvious adverse effect on the pregnancy. Early reports suggested a relationship between levodopa during

Pregnancy

and fulminant hepatitis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Levodopa crosses the human placenta, and limited study suggests it achieves an F:M ratio approaching unity. While some studies show that levodopa concentrates in the fetal brain and thus has the potential to affect fetal neuronal development, the majority of studies reveal no evidence of teratogenicity. Rodent studies are generally reassuring, without evidence of teratogenicity, though IUGR occurs at high doses.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Levodopa is excreted into human breast milk, but the kinetics remain to be elucidated. While it suppresses prolactin release and thus, theoretically, may interfere with lactation, the suckling stimulus seems to override any inhibitory effect on prolactin release.

Pregnancy

. Levofloxacin is indicated for the treatment of mild, moderate, and severe infections caused by a wide variety of susceptible microorganisms. There are no adequate reports or well-controlled studies of levofloxacin in pregnant women. Compared to other quinolones, levofloxacin has fewer adverse GI or CNS events and is minimally phototoxic. Levofloxacin should not be used for the treatment of gonorrhea because of the growing prevalence of resistant strains. Recent studies report increased sensitivity of Chlamydia trachomatis to quinolone medication. Vaginal candidiasis is more frequently associated with quinolone use than with other antibiotics. 583

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Less than 4% of maternal levofloxacin and ofloxacin crosses the isolated perfused human placenta. Intracompartmental clearance has not been detailed to date. Animal studies (mice, dogs, rabbits) reveal that several quinolones are associated with a juvenile arthropathy, and it is this toxicity that has lead to their restricted use in pregnant women. However, not all quinolones have the same potency on cartilage growth. Further, the use of quinolones during the 1st trimester of human

Pregnancy

has not been associated with an increased risk of malformations or musculoskeletal conditions. Rodent studies with levofloxacin are reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. IUGR was noted.

Breastfeeding

At steady state, peak levofloxacin exposure in breast milk approximates 8mcg/ml 5h after dosing. Elimination pharmacokinetics followed the anticipated pattern. Thus, peak levofloxacin concentrations in human breast milk are similar to levels attained in plasma. However, Breastfeeding mothers who take levofloxacin will expose their infants to levofloxacin in concentrations below those being studied in the pediatric population.

Pregnancy

. Levorphanol has properties similar to morphine, but is 4-6? more potent. There is no published experience during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Its chemical structure suggests levorphanol will rapidly cross the placenta. Adolescent rodents exposed prenatally to morphine are tolerant to its analgesic effect. This tolerance also occurs when the rats are exposed to levorphanol, a morphine congener, but not by its analgesically inactive isomer, dextromethorphan. 585

Breastfeeding

There is no published experience in nursing women. It is unknown whether levorphanol enters human breast milk.

Pregnancy

. Lidocaine has been used for decades for paracervical/pudendal blocks and perineal infiltration prior to episiotomy. Buffered products reduce the pain of infiltration. However, sprayed lidocaine is not effective for perineal anesthesia. Allergies are rare. It is often used for spinal anesthesia (saddle block) without epinephrine or epidural anesthesia with epinephrine. The prevalence of maternal hypotension may be higher with lidocaine than with bupivacaine. Both the quality and the duration of 590 anesthesia are improved by the addition of fentanyl. The topical application of 2% lidocaine gel decreases perineal pain in women with genital herpes. Lidocaine is a second option for the treatment of ventricular arrhythmias after failed electrical cardioversion.

Fetal Health

Lidocaine rapidly crosses the human placenta, and its elimination t/2 after birth approximates 3h. Lidocaine administered by the perineal route has a Tmaxof 15min, significantly lower than when the drug is administered peridurally; M:F ratios in this instance approximate 1:2 at the time of delivery. It is not placenta-bound. The results of neurobehavioral exams of newborns whose mothers received continuous epidural analgesia are conflicting. Some suggest a decrease in muscle strength and tone, while others find no effect. Lidocaine can potentially produce neonatal CNS depression and seizures. There are no reports of associated malformations. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Lidocaine is excreted into breast milk, but the maternal systemic levels are low. Considering the dose and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. There are 2 main antibiotics in the lincosamide family: lincomycin and clindamycin. Because lincomycin has been associated with severe colitis that may end fatally, it should be reserved for serious infections where less toxic antimicrobial agents are ineffective. There are no adequate reports or well- controlled studies of lincomycin in pregnant women, in whom clindamycin is commonly used.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether lincomycin crosses the human placenta. Rodent teratogen studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Lincomycin is excreted into human breast milk, achieving concentrations of 0.5-2.4mcg/ml. Even if a term 592 breastfed newborn had 100% absorption, the daily dose would be <2mg.

Pregnancy

. Lindane (g-hexachlorocyclohexane) is a popular OTC treatment for scabies. The number of suspected adverse reactions is small considering over 10 million ounces of 1% lindane are sold yearly. Almost all suspected adverse drug reactions involve misuse. There are no adequate reports or well-controlled studies of lindane in pregnant women. However, lindane is stored in fat, and rodent studies describe a reduction in uterine gap junction synthesis and, as a result, incoordination of uterine contractions.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Lindane likely crosses and is stored in the human placenta. It is a known neurotoxin. One report describes a suicide attempt with oral ingestion at 16w followed immediately by fetal death and vaginal bleeding. Fortunately, the maternal systemic concentrations after topical application (cream or shampoo) are low. An increased prevalence of IUGR has been suggested. Transfer across the rabbit placenta occurs but is inefficient. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Lindane transiently reduces fetal serum T4in sheep.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Lindane is excreted into human milk at low concentrations (0-113ppb) and may also be present due to environmental contamination; it is unlikely the neonate would ingest a clinically relevant amount. However, if this is a concern, the neonate may be bottle fed for 2d.

Pregnancy

. Linezolid is a member of a new class of synthetic antibiotics, the oxazolidinones. It is also a nonselective MAOI. This family of drugs is useful in the treatment of aerobic gram-positive and -negative bacteria infections. There is no published experience with linezolid during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether linezolid crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity is noted only at doses causing maternal toxicity.

Breastfeeding

There is no published experience in nursing women. It is unknown whether linezolid enters human breast milk. It is excreted into rat milk, achieving an M:P ratio near unity.

Pregnancy

. Liothyronine is synthetic T3. Myxedema coma is a potentially lethal manifestation of hypothyroidism. Patients with suspected myxedema coma should be immediately admitted to an ICU for aggressive pulmonary and CV support. Most authorities recommend treatment with IV levothyroxine rather than IV liothyronine. Hydrocortisone is also administered until coexisting adrenal insufficiency is excluded. Advanced age, cardiac complications, and high-dose thyroid hormone replacement (>500mcg/d) are associated with a fatal outcome within 1mo of treatment. Amiodarone-induced hypothyroidism may also be life-threatening, and thyroid function should be tested before and during amiodarone therapy. There are no adequate reports or well-controlled studies of liothyronine in pregnant women. There are no reports of myxedema coma during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies of liothyronine in human fetuses. Transfer of natural T3across the human placenta is low but physiologically relevant.

Breastfeeding

It is unknown whether liothyronine enters human breast milk. However, several studies conclude the amount of thyroid hormone present in human milk is too low to clinically affect the neonate. It is unknown whether supplementation increases the level.

Pregnancy

. Liotrix is synthetic microcrystalline levothyroxine (T4) and synthetic microcrystalline liothyronine (T3) combined in a 4:1 ratio. There are no adequate reports or well-controlled studies of liotrix in pregnant women (see Levothyroxine, Liothyronine).

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses (see Levothyroxine, Liothyronine).

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether liotrix enters human breast milk. (See Levothyroxine, Liothyronine.)

Pregnancy

. There are no adequate reports or well-controlled studies of lisinopril in pregnant women. In general, inhibitors of the renin- angiotensin system are contraindicated throughout pregnancy. The lowest dose effective should be used when lisinopril is required during

Pregnancy

for BP control.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Lisinopril crosses the human placenta. No adverse fetal effects are reported following 1st trimester exposure. However, such adverse events are well-documented after the ingestion of other ACEIs. Later exposure is associated with cranial hypoplasia, anuria, reversible or irreversible renal failure, death, oligohydramnios, prematurity, IUGR, and PDA. The mechanism of renal dysfunction is likely related to fetal hypotension and prolonged decreased glomerular filtration. If oligohydramnios is detected, lisinopril should be discontinued unless lifesaving for the mother. Antenatal surveillance should be initiated (e.g., BPP) if the fetus is potentially viable. Oligohydramnios may not appear until after the fetus has irreversible injury. Neonates exposed in utero to ACEIs should be observed closely for hypotension, oliguria, and hyperkalemia. If oliguria occurs despite adequate pressure and renal perfusion, exchange transfusion or peritoneal dialysis may be required.

Breastfeeding

There is no published experience in nursing women. It is unknown whether lisinopril enters human breast milk. Other ACEIs (e.g., captopril) are excreted in the milk at low concentrations.

Pregnancy

. Lithium is used for the treatment of psychiatric disorders. It is typically inadequate for the rapid control of acute mania; antipsychotics, divalproex, or sedatives are commonly used, with or without lithium in these instances. The usefulness of lithium lies in the long-term prevention of recurrent mania and bipolar depression and in reducing risk of suicidal behavior. Among patients treated for a bipolar disorder, the risk of a suicide attempt is lower during treatment with lithium than it is with divalproex.

Pregnancy

and especially the puerperium are times high risk for recurrence of bipolar disease. Recommendations during

Pregnancy

include discontinuing therapy for at least the 1st trimester, switching to an agent with a less controversial profile (e.g., tricyclics), using smaller doses of lithium, and avoiding sodium restriction or diuretics while under treatment. However, discontinuation during

Pregnancy

of mood stabilizer, particularly abruptly, carries a high risk for new morbidity in women with bipolar disease, especially for early depressive and dysphoric states. This risk is reduced markedly by continued mood stabilizer treatment. Treatment planning for pregnant women with bipolar disease should consider not just the relative risks of fetal exposure but also the high risk of recurrence and morbidity associated with stopping therapy. The dose used should be titered to maintain a serum level between 0.5-1.2mEq/L. Toxicity develops between 1.5 and 2.0mEq/L. Ideally, the drug should be tapered gradually over a month. Lithium levels should be monitored weekly after 35w gestation, and therapy either discontinued or decreased by1=4 2-3d before delivery. 601

Fetal Health

Lithium crosses the placenta; the F:M ratio approximates 1 across a wide range of maternal concentrations (0.2-2.6mEq/L). Infants with higher lithium concentrations (>0.64mEq/L) at delivery have significantly lower Apgar scores, longer hospital stays, and higher rates of CNS and neuromuscular complications. Withholding lithium therapy for 24-48h before delivery decreases the maternal lithium concentration an average of 0.28mEq/L. Several studies note an increased prevalence of Ebstein?s anomaly, though this was not confirmed in a prospective, multicenter study. The main effects attributable to lithium are cardiac malformations and increased birth weight. A targeted ultrasound performed by a fetal medicine expert is suggested. Fetuses of depressed mothers are more active during midgestation and exhibit lower baseline HRs and move less during late-term vibratory stimulation. Midgestation heightened activity and late- term diminished responsivity may be a prenatal manifestation of the ??general adaptation syndrome.?? SSRIs increase middle cerebral artery velocity while lithium decreases it. Neonatal complications often attributed to lithium include poor respiratory effort and cyanosis, rhythm disturbances, nephrogenic diabetes insipidus, thyroid dysfunction and goiter, hypoglycemia, hypotonia and lethargy, polyhydramnios, hyperbilirubinemia, and large-for-gestational-age infant. As a result, the delivery of a mother taking lithium should be considered a high-risk delivery. However, the results of long-term follow-up studies are reassuring as are the most recent epidemiologic studies. Animal studies using doses producing serum levels similar to therapeutic human levels have not reported any abnormalities, though higher doses have produced exencephaly, skeletal and craniofacial defects, and abnormalities of blood vessel development. Experiments with other vertebrates suggest lithium affects dorsoventral specification and inhibition of vasculogenesis. Both these effects can be prevented by pretreatment with myoinositol, indicating that lithium interferes with the phosphatidylinositol cycle.

Breastfeeding

Lithium is excreted into human milk and can be measured in the nursing newborn. Maternal serum, breast milk, and infant serum daily trough levels of lithium are reported to average 0.76, 0.35, and 0.16mEq/L, respectively, each level lower than the preceding by approximately1=2. In this study, no serious adverse events were observed, and elevations of TSH and BUN/Cr were few, minor, and transient.

Pregnancy

. There is no published experience with lodoxamine during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether lodoxamine crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Considering the dose and route, 604 it is unlikely the maternal systemic concentration will reach a clinically relevant level.

Breastfeeding

There is no published experience in nursing women. It is unknown whether lodoxamine enters human breast milk. However, considering the dose and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. This quinolone has poor efficacy against anaerobic infections. There are no studies of lomefloxacin in pregnant women. Superior agents are usually available.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether lomefloxacin crosses the human placenta. Animal studies (mice, dogs, rabbits) report that several quinolones lead to arthropathy, and this toxicity resulted in the recommended restricted use in pregnant women. However, not all quinolones have the same potency on cartilage growth. Further, the use of quinolones during the 1st trimester of

Pregnancy

is not associated with an increased risk of malformations or musculoskeletal conditions. Rodent and monkey studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. There was evidence of embryo and fetal toxicity at high doses.

Breastfeeding

There is no published experience with lomefloxacin in nursing women. Other quinolones are excreted into human breast milk.

Pregnancy

. Loperamide is a popular and effective agent for the treatment of diarrhea (??traveler?s diarrhea??) and associated symptoms. It reduces the incidence of Side effects include necrotizing enterocolitis, paralytic ileus, drowsiness, dizziness, dry mouth, abdominal pain, abdominal distention, constipation, N/V, fatigue, and skin rash.

Fetal Health

Prospective human studies suggest that the use of loperamide during

Pregnancy

is not associated with an increased risk of major malformations. However, a recent registry report observed an increase in hypospadias when used during early pregnancy. Breastfeeding Although there are no adequate reports or well-controlled studies in nursing women, loperamide is generally considered safe for

Pregnancy

. Loracarbef is used to treat lower respiratory tract infections, GU tract infections, skin infections, and septicemia, and for surgical prophylaxis. Though cephalosporins are usually considered safe during pregnancy, there is no published experience with loracarbef during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies of loracarbef in human fetuses. Other cephalosporins cross the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether loracarbef enters human breast milk. Most cephalosporins are excreted into breast milk.

Pregnancy

. Loratadine is a 2nd-generation antihistamine with minimal sedating effect. It is a first-line agent for the treatment of allergic rhinorrhea. There are no adequate reports or well-controlled studies of loratadine in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether loratadine crosses the human placenta. Prospective human studies reveal no adverse outcomes. In 2002, a Swedish study observed that, among male infants born to women who took loratadine for seasonal allergies, the prevalence of hypospadias was twice that of the general population. However, the CDC recently analyzed data from the National Birth Defects Prevention Study and determined there was no increased risk for 2nd or 3rd degree hypospadias in the 609 male offpring of women who used loratadine in early pregnancy. This conclusion is confirmed by a recent Danish study. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Loratadine and its active metabolite, descarboethoxyloratadine, pass easily into human breast milk, achieving concentrations almost equivalent to maternal plasma. However, the total dose absorbed by the Breastfeeding neonate is <1%.

Pregnancy

. There is a growing appreciation that the purported risks of lorazepam during

Pregnancy

are smaller than first thought. Women in need of the therapy should not be denied it solely because of the pregnancy. Although nonpharmacologic approaches to the treatment of insomnia are first-line therapy, intermediate-acting benzodiazepines such as lorazepam and temazepam may be useful in some circumstances. Lorazepam reverses the hypothermia associated with neuraxial anesthesia utilizing bupivacaine, morphine, and fentanyl.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Lorazepam crosses the human placenta. High peak concentrations are avoided by dividing the daily dose into 2 or 3. While there are many studies of benzodiazepine use in human pregnancy, data on teratogenicity and effects on postnatal development and behavior are limited and conflicting. Early studies suggested that 1st trimester exposure to benzodiazepines was associated with an increased risk of facial clefts and cardiac malformations. Subsequent studies contradicted that conclusion, finding no clear evidence of an increase in either the overall incidence of malformations or any particular type of defect. Benzodiazepine use in the 3rd trimester or during labor may cause the floppy infant syndrome or neonatal withdrawal. There is no increase in jaundice at term. Rodent studies are for the most part reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. In other rodent studies, prenatal exposure to some benzodiazepines is associated with behavioral and neurochemical alterations in the early postnatal period that may persist into adulthood. Studies in humans document an effect at least up to 18mo of age.

Breastfeeding

Lorazepam is excreted into human breast milk. It has been estimated the breastfed neonate ingests <1% of the maternal dose, a dose that should be clinically insignificant. Using the lowest effective quantity in divided doses to minimize drug peaks could further minimize any theoretic risk.

Pregnancy

. There are no adequate reports or well-controlled studies of lovastatin in pregnant women. The limited information available on the effect of HMG-CoA reductase inhibitors on

Pregnancy

suggests similar outcomes as the general, nonexposed population. Hypercholesterolemia is a chronic problem. Discontinuation of lovastatin during

Pregnancy

is unlikely to increase maternal morbidity.

Fetal Health

Cholesterol and other products of the cholesterol biosynthesis are essential components for fetal development. There are no adequate reports or well-controlled studies of lovastatin in human fetuses. It is unknown whether it crosses the human placenta, and there is limited follow-up study. Lovastatin is lipophilic and should equilibrate between maternal and fetal compartments. Retrospective series tend to raise the most suspicion. For example, one review of 214

Pregnancy

exposures to one of several statins with 70 informative cases noted 31 adverse outcomes, including 22 cases with structural defects, 4 cases of 612 IUGR, and 5 fetal deaths. Cerivastatin and lovastatin were associated with 4 reports of severe midline CNS defects; simvastatin, lovastatin, and atorvastatin were each associated with reports of limb deficiencies. None were reported after exposure to pravastatin, which is poorly transported across the placenta. These authors concluded that statins may have secondary effects on sterol-dependent morphogens such as Sonic Hedgehog. A more recent survey included 225 prospective outcomes reported for lovastatin specifically: 154 live-born infants, 49 elective abortions, 18 spontaneous abortions, and 4 fetal deaths. Six congenital anomalies were reported: chromosomal translocation, trisomy 18, hypospadias, duodenal atresia, cleft lip, and skin tag. The rate of congenital anomalies (congenital anomalies/live births plus fetal deaths) was 3.8%, which is similar to the background population rate (3.2%; relative ratio, 1.21; 95% 1-sided upper CI, 2.02). Skeletal abnormalities were also noted when the administered dose of lovastatin exceeded 40the MRHD. Some animal studies suggest the statin drugs might be neuroprotective against hypoxic/ischemic stroke.

Breastfeeding

There is no published experience in nursing women. Small quantities of lovastatin apparently enter human breast milk, but the kinetics are unknown. Statin drugs inhibit prolactin release in the rat brain, and theoretically could interfere with the initiation of lactation.

Pregnancy

. Loxapine is a tranquilizer indicated for the management of the manifestations of psychotic disorders. Galactorrhea is a common complication. There are no adequate reports or well-controlled studies of loxapine in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether loxapine crosses the human placenta. Rodent studies are reassuring, but are limited.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Loxapine is excreted into human breast milk, but the kinetics have yet to be elucidated.

Pregnancy

. Lypressin is indicated for the treatment of diabetes insipidus. It is a synthetic version of the natural porcine compound. There is no published experience with lypressin during pregnancy. It is a powerful vasoconstrictor when applied to isolated vessels and induces contractions in isolated myometrium from humans.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether lypressin crosses the human placenta. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There is no published experience in nursing women. It is unknown whether lypressin enters human breast milk. Lypressin stimulates mammary ejection pressure in sheep.

Pregnancy

. There are no adequate reports or well-controlled studies of magnesium chloride in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies of magnesium chloride in human fetuses. Magnesium administered parenterally to the mother crosses the placenta. Rodent studies are reassuring.

Breastfeeding

Magnesium is normally present in human breast milk, and its concentration stable throughout the 1st year of lactation. It is unknown whether magnesium chloride increases the magnesium content of breast milk. Considering the indications, limited use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Magnesium citrate reduces the frequency of night leg cramps in nonpregnant patients. There are no adequate reports or well- controlled studies of magnesium citrate in pregnant women. Its use during

Pregnancy

increases serum magnesium.

Fetal Health

There are no adequate reports or well-controlled studies of magnesium citrate in human fetuses. Magnesium ions freely cross the placenta.

Breastfeeding

Magnesium is normally present in human breast milk, and its concentration stable throughout the 1st year of lactation. It is unknown whether magnesium citrate increases the magnesium content of breast milk. Considering the indications and dosing, limited use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. There are no adequate reports or well-controlled studies of magnesium oxide in pregnant women. Obstetricians have used oral magnesium as a tocolytic agent without demonstrable efficacy. It has also been advocated as a neuroprotectant for the acutely hypoxic fetus and to prevent preeclampsia. Neither indication can be substantiated.

Fetal Health

There are no adequate reports or well-controlled studies of magnesium oxide in human fetuses.

Breastfeeding

Magnesium is normally present in human breast milk, and its concentration stable throughout the 1st year of lactation. It is unknown whether magnesium oxide increases the magnesium content of breast milk.

Pregnancy

. Magnesium sulfate is excreted by the kidney, with 90% of the dose excreted during the first 24h after an IV infusion. The pharmacokinetic profile of magnesium sulfate after IV administration is best described by a 2-compartment model with a rapid distribution (alpha) phase, followed by a relatively slow beta phase of elimination. The clinical effect and toxicity of magnesium is linked to its plasma concentration. A decreased GFR may lead to toxicity if not monitored closely. Use only1=2 the usual load when the plasma Cr exceeds 1.3mg/dl. DTRs are decreased as the concentration exceeds 4mEq/L; they are lost as the level approaches 10mEq/L. Potentially, lethal respiratory depression may occur at 12-15mEq/L. Recent investigation suggests the measurement of total magnesium is not adequate for titration in women with either preeclampsia or preterm labor as there is poor correlation between total magnesium and the physiologically active ionized magnesium. Calcium gluconate should always be readily available to counteract potential serious signs of magnesium intoxication. Preeclampsia remains a leading cause of maternal and perinatal morbidity and death. Randomized trials demonstrate magnesium sulfate infusion halves the risk of eclampsia and is superior to both phenytoin and diazepam for the prevention of recurrent eclamptic seizures. The anticonvulsant effect is probably exerted on the cerebral cortex. It is also the drug of choice for the control of seizures. Magnesium sulfate is NOT an effective antihypertensive, though Mg2+concentrations between 2 and 4mmol/L produce greater than half the maximal lowering of systolic and diastolic pressures. There remains controversy as to whether magnesium sulfate is beneficial for the treatment of mild preeclampsia. A recent analysis concluded that the risks and benefits of magnesium in this patient population counterbalance each other. Although a no-magnesium strategy results in a 15% 619 reduction in neonatal mortality and avoids maternal drug toxicity, it leads to a 2-fold increase in maternal death and more neurologically compromised neonates compared to empiric magnesium. The clinical decision to use magnesium in women with mild preeclampsia for seizure prophylaxis should be determined by the physician or institution, considering patient values or preferences and the unique risk:benefit trade-off of each strategy. However, magnesium sulfate treatment clearly does not prevent the worsening of preeclampsia during labor. Approximately 10-15% of eclamptic women convulse despite prophylaxis. An additional 2g loading dose is recommended if a woman convulses while receiving magnesium sulfate for the prevention of eclampsia. Magnesium sulfate may also be administered IM. Prospective studies comparing magnesium levels achieved with continuous IV infusion and IM reveal that therapeutically effective levels are achieved with both. Magnesium sulfate neither prolongs labor nor increases the oxytocin requirement in preeclamptic women. Magnesium sulfate is often continued for at least 24h postpartum, but there is little scientific support for the practice. The duration of therapy may be individualized using maternal diuresis (>200ml/h for at least 2h) as evidence the associated vasospasm has resolved. In one study, women with mild preeclampsia received shorter courses o

Breastfeeding

Some case reports describe engorgement and galactorrhea during tocolysis with IV magnesium sulfate. The mechanism remains unknown. Symptoms gradually subside after discontinuation. Magnesium is normally present in human breast milk, and its concentration stable throughout the 1st year of lactation. It is unknown whether magnesium sulfate increases the magnesium content of breast milk. Considering the indication and dosing, limited use is unlikely to pose a clinically significant risk to the

Breastfeeding

neonate.

Pregnancy

. Mannitol is an osmotic diuretic. It is confined to the extracellular space after IV administration and is rapidly excreted by the kidneys (80% within 3h). There are no adequate reports or well-controlled studies of mannitol in pregnant women. The published experience is limited to case reports of women often undergoing surgery for causes unrelated to

Pregnancy

(intracranial hemorrhage or brain tumors) or for hypermagnesemia. It has also 623 been used for the treatment of posterior, reversible encephalopathy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Mannitol crosses the human placenta by diffusion. Rodent teratogenicity studies have not been performed. Studies of pregnant ewes reveal that maternal hyperosmolality influences the fetal arginine vasopressin secretion and renal function, and thus the amount of AF.

Breastfeeding

There is no published literature in nursing women. It is unknown whether mannitol enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of maprotiline in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether maprotiline crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Rodent and chick studies suggest maprotiline is less embryo and organ toxic than imipramine and amitriptyline.

Breastfeeding

There is no published experience in nursing women. It is unknown whether maprotiline enters human breast milk.

Pregnancy

. Mazindol behaves like an amphetamine. Its efficacy in obese nonpregnant women is at best modest, and tolerance develops. There is no published experience during pregnancy, nor are there any indications for its use.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether mazindol crosses the human placenta. Rodent studies suggest an increase in rib abnormalities at multiples of the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether mazindol enters human breast milk.

Pregnancy

. Treatment of reproductive-age women is strongly recommended in areas of widespread hookworm infection and its related anemia. In some endemic areas, treatment of all pregnant women after the 1st trimester effectively reduces the incidences of IUGR and perinatal death.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether mebendazole crosses the human placenta. Congenital helminthic infection in humans is rare. No increase in risk for congenital malformation or other adverse outcomes was noted in the largest prospective study with 140 1st trimester exposures. There are no reported sequelae from 2nd or 3rd trimester exposure. Rodent studies suggest mebendazole is embryotoxic and teratogenic at fairly low doses.

Breastfeeding

There is no published experience in nursing women. It is unknown whether mebendazole enters human breast milk.

Pregnancy

. There is no published experience with mecamylamine during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies of mecamylamine in human fetuses. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There is no published experience in nursing women. It is unknown whether mecamylamine enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of mechlorethamine in pregnant women. Hodgkin?s disease does not affect the normal progress of pregnancy. Termination of

Pregnancy

is usually unnecessary. Based on limited published experience, mechlorethamine may be used during

Pregnancy

with a good outcome. Women treated during childhood or adolescence may experience decreased gonadal function.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether mechlorethamine crosses the human placenta. Children of women treated for hematologic malignancies during

Pregnancy

with a variety of cytotoxic agents, including mechlorethamine, have normal birth weight as well as normal learning and educational performances. There is no increase in the prevalence of acute leukemia or congenital, neurologic, and psychological abnormalities. Thus, chemotherapy at full doses administered during

Pregnancy

even during the 1st trimester can end with a good outcome. Mechlorethamine is teratogenic in rodents.

Breastfeeding

There is no published experience in nursing women. It is unknown whether mechlorethamine enters human breast milk.

Pregnancy

. Meclizine effectively reduces N/V associated with emergency hormonal contraception (Yuzpe regimen). There are no adequate reports or well-controlled studies of meclizine in pregnant women. It is commonly used in several European countries for the treatment of 1st trimester N/V.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether meclizine crosses the human placenta. A large clinical experience reveals little evidence that meclizine is a significant human teratogen. A population- based study inthat included more than 16,000 1st trimester exposures actually reported improved

Pregnancy

outcomes compared to the nonexposed population. Rodent studies conducted at 25-50the MRHD reveal cleft lip and palate.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether meclizine enters human breast milk.

Pregnancy

. Meclofenamate is a nonsteroidal agent with anti-inflammatory, analgesic, and antipyretic activities. It has little effect on human platelet function. There are no adequate reports or well-controlled studies of meclofenamate in pregnant women. In rodents, meclofenamate induces luteolysis as indicated by the drop in maternal progesterone after administration. Luteolysis is followed by spontaneous labor. In contrast, in vitro studies demonstrate meclofenamate inhibits myometrial contractility. Meclofenamate is a popular analgesic for the treatment of postpartum pain after vaginal delivery.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether meclofenamate crosses the human placenta. Similar-class agents do cross, cause fetal ductal constriction and decreased fetal urination. Because of the potential for premature closure of the fetal ductus arteriosus after maternal use of NSAIDs, chronic mefenamic acid treatment during

Pregnancy

is not recommended without fetal monitoring. Fetal exposure should be minimized until completion of future studies since meclofenamate may affect fetal breathing movements and pulmonary vascular resistance. Rodent studies reveal that meclofenamate, like aspirin and other NSAIDs, can cause fetotoxicity and minor skeletal malformations (e.g., supernumerary ribs, delayed ossification) but no major teratogenicity.

Breastfeeding

There is no published experience in nursing women. Meclofenamate enters human breast milk, though the kinetics remain to be elucidated. 631

Pregnancy

. Medroxyprogesterone is a popular and effective (0.42/1000 woman-years) contraceptive; irregular bleeding and amenorrhea are the most common Side effects include thromboembolism, stroke, MI, hepatic adenoma, breast cancer, gallbladder disease, cholestatic jaundice, hypertension, stroke, amenorrhea, N/V, breast tenderness, weight gain, headache, edema, depression, rash, pruritus, libido changes, appetite changes, acne, hirsutism, galactorrhea, alopecia, and optic neuritis.

Fetal Health

There are no adequate reports or well-controlled studies of medroxyprogesterone in human fetuses. In utero exposure of male fetuses to progestational agents may double the risk of hypospadias. While there are insufficient data to quantify the risk for the female fetus, some progestational agents may cause mild virilization of the external genitalia. Defects outside the external genitalia are not noted in either humans or rodents. 1st trimester exposure is an indication for a detailed anatomic ultrasound between 18 and 22w. Breastfeeding Trace amounts of medroxyprogesterone are excreted into human breast milk. It does not appear to either suppress lactation or affect the nursing newborn. It is typically given for contraception 3d after delivery since progesterone withdrawal may be one stimulus for the initiation of lactogenesis.

Pregnancy

. Mefenamic acid is a nonsteroidal agent with anti-inflammatory, analgesic, and antipyretic action. There are no adequate reports or well-controlled studies of mefenamic acid in pregnant women. In one small, randomized trial, the prevalence of preterm labor was significantly reduced by mefenamic acid compared with placebo. This observation has not subsequently been tested adequately. If the effect of mefenamic acid is similar to other NSAIDs, it is unlikely to be effective for the stated indication. Mefenamic acid rapidly decreases uterine contractility in women with dysmenorrhea.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Mefenamic acid crosses the human placenta, achieving an F:M ratio approximating 0.32 in the 2nd trimester. There are case reports of ductal closure reported as with other NSAIDs. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than 634 those used clinically. Embryotoxicity is noted in some species. Because of the potential for premature closure of the fetal ductus arteriosus after maternal use of NSAIDs, chronic mefenamic acid treatment during

Pregnancy

is not recommended without fetal monitoring.

Breastfeeding

The trace amounts of mefenamic acid excreted into breast milk pose no clinical risk to the nursing infant.

Pregnancy

. Malaria remains an important cause of maternal and perinatal morbidity and mortality in endemic countries. P. falciparum drug resistance increasingly limits the effectiveness of antimalarial therapy. Mefloquine is the most effective agent for the prevention of chloroquine-resistant falciparum malaria. The WHO favors mefloquine prophylaxis in pregnant women from 16w onward. Mefloquine and quinine are the only antimalarials generally available for the treatment of drug- resistant P. falciparum during pregnancy. Prospective studies show mefloquine (25mg/kg) in combination with artesunate (4mg/kg/d for 3d) is more effective than quinine (10mg/kg q8h) for the treatment of multidrug-resistant falciparum malaria during pregnancy. Many of the adverse effects of mefloquine reflect primary hepatic damage or symptomatic thyroid disturbances, which might occur either independently or as a secondary consequence of the hepatocellular injury. Routine intermittent treatment of women in endemic locales has been suggested.

Fetal Health

Prophylactic (250mg/w) mefloquine during early

Pregnancy

is not associated with an increased risk of malformations and is not an indication for

Pregnancy

termination. Similarly, 2nd trimester exposure is not associated with adverse reactions. Mefloquine is associated with an increased risk of stillbirth but not abortion, IUGR, neurologic retardation, or congenital malformations. Rodent studies reveal that mefloquine at high doses is teratogenic and embryotoxic.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. The detectable amounts of drug identified in the milk of mothers receiving mefloquine are too small to be clinically relevant. 636

Pregnancy

. Megestrol is a synthetic, progestational drug. It is used as an implantable contraceptive. There are no adequate reports or well- controlled studies of megestrol in pregnant women, nor are there any indications for its use. Many case reports document successful

Pregnancy

in women with endometrial cancer whose uterus was preserved by megestrol. As a treatment for weight loss in cancer patients, megestrol should be started only after other treatable causes are sought and addressed.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether megestrol crosses the human placenta. There are case reports of abnormalities, including hypospadias.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Small quantities of megestrol are excreted into human breast milk. However, megestrol has no clinically relevant effect on breast milk when used for contraception.

Pregnancy

. There are no adequate reports or well-controlled studies of melatonin in pregnant women. Melatonin is a natural hormone (N-acetyl-5-methoxytryptamine) produced by the pineal gland with antioxidant properties. Its secretion is stimulated by the dark and inhibited by light. Secretion disturbances have been associated with depression. Rodent studies suggest that melatonin is involved in the initiation of parturition without having a direct effect on progesterone secretion. In humans, melatonin may also modulate myometrial function, as receptors are present.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Melatonin rapidly crosses the isolated human placenta equal to the freely diffusible marker antipyrine. It stimulates glutathione peroxidase in the human chorion and inhibits the vasospastic effects of oxidized lipids. It also crosses the rodent placenta, and fetal rodents respond to the maternal melatonin rhythm. Melatonin may offer some protection for ischemia/reperfusion-induced oxidative mitochondrial damage to the fetal rat brain.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. In both human and rodent breast milk, melatonin is undetectable in the light but increases rapidly after dark. The M:P ratio ranges from 0.35 to 0.8, and melatonin is believed responsible for shifting the newborn to the circadian rhythm of the mother. 639

Pregnancy

. Meloxicam is a nonsteroidal agent with anti-inflammatory, analgesic, and antipyretic activities. There is no published clinical experience during pregnancy. In the ewe, meloxicam is an inhibitor of uterine contractions. It, with indomethacin, is a modest inhibitor of preterm labor in rats treated with LPS. In vitro, meloxicam relaxes myometrial strips from pregnant and nonpregnant women, but is less potent than celecoxib.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Meloxicam crosses the human placenta. The administration of high doses to rodents is associated with cardiac septal defects and embryotoxicity. Meloxicam attenuates RU486-stimulated labor in sheep. Because of the potential for premature closure of the fetal ductus arteriosus after maternal use of NSAIDs, chronic meloxicam treatment during

Pregnancy

is not recommended without fetal monitoring.

Breastfeeding

There is no published experience in nursing women. It is unknown whether meloxicam enters human breast milk. It does enter rodent milk.

Pregnancy

. Melphalan is an alkylating agent. While methotrexate is the primary choice for uncomplicated malignant trophoblastic disease, occasional resistance to methotrexate requires alternative drug regimens that may include melphalan (e.g., melphalan, actinomycin D, and methotrexate). These regimens are more frequently associated with life-threatening hematologic toxicity compared to those regimens that include methotrexate. Women cured of either trophoblastic disease or ovarian cancer (usually stage 1A-C) using a drug regimen that includes melphalan can have successful pregnancies. Melphalan is also used for the treatment of primary thrombocythemia and for marrow conditioning prior to allogeneic marrow transplantation. There are no adequate reports or well-controlled studies of melphalan in pregnant women. There are only case reports of its use during an ongoing pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether melphalan crosses the human placenta. Rodent studies reveal both embryotoxicity and teratogenicity. Anomalies include CNS and skeletal defects.

Breastfeeding

There is no published experience in nursing women. It is unknown whether melphalan enters human breast milk.

Pregnancy

. There is no published experience with mepenzolate during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether mepenzolate crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of higher doses than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether mepenzolate enters human breast milk.

Pregnancy

. Meperidine is a synthetic narcotic qualitatively similar to morphine. It is metabolized to another active form, normeperidine. Historically, meperidine was perhaps the most commonly used parenteral opioid during labor for pain relief. Well-designed studies demonstrate that the incidence of cesarean delivery in nulliparous women with epidural analgesia is similar to IV meperidine but, with superior analgesia, less maternal sedation and no need for neonatal naloxone as with meperidine. When used for early labor analgesia, meperidine increases the prevalence of neonatal acidemia. It does not improve outcome 644 when given for dystocia. Meperidine does not have in vitro a significant effect on the spontaneous contractions of gravid human myometrium. Postoperatively, PCEA with meperidine offers high-quality pain relief with few Side effects include respiratory arrest and depression, cardiac arrest, tachydysrhythmias, dependency, abuse, vomiting, sweating, shock, agitation, disorientation, euphoria, dysphoria, weakness, dry mouth, flushing, visual disturbances, constipation, biliary tract spasm, palpitation, hypotension, syncope, pruritus, skin rashes, and pain at the site of injection.

Fetal Health

Meperidine crosses the human placenta. It significantly decreases the number of FHR accelerations intrapartum, and is associated with insufficient fetomaternal gas exchange and fetal acidemia. Meperidine achieves its highest concentration in fetal tissues 2-3h after administration, correlating with the clinical observation that the maximal risk of neonatal depression occurs 2-3h after maternal injection. Respiratory depression requiring resuscitation at delivery is a risk. The interval before neonatal respiration becomes sustained increases if meperidine is given more than 1h before delivery. The greater the drug-to-delivery interval, the higher the fetal concentration of normeperidine, and the lower the newborn?s performance on the Brazelton Neonatal Behavioral Assessment Scale. Spontaneous behavior and cognitive performance in exposed rhesus monkeys at 3-12mo of age is altered by meperidine. Breastfeeding Meperidine is excreted into human breast milk, with peak levels occurring about 2h after administration. While a single dose of meperidine has little impact on the nursing infant, repeated administration negatively affects the newborn. Nursing infants repeatedly exposed to morphine are more alert and oriented than those exposed repeatedly to meperidine. This makes morphine the preferred narcotic for lactating mothers.

Pregnancy

. Mephentermine is a synthetic sympathomimetic used for treatment of hypotension. It increases stroke volume and thus increases both systolic and diastolic BP. There is also a variable degree of peripheral vasoconstriction. Mephentermine increases HR by the release of epinephrine. There are no adequate reports or well- controlled studies of mephentermine in pregnant women. It has been used during

Pregnancy

to restore or support uteroplacental blood flow after spinal or epidural analgesia. Though a recent RCT concluded ephedrine and mephentermine had similar efficacy, it has largely been abandoned in favor of ephedrine.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether mephentermine crosses the human placenta. Rodent teratogenicity studies have not been performed. Studies in animals and humans reveal fetal hypoxia after mephentermine presumably secondary to uterine artery constriction and decreased uterine blood flow. Transient fetal hypertension (mean arterial BP >20% of control) is also reported.

Breastfeeding

There is no published experience in nursing women. It is unknown whether mephentermine enters human breast milk.

Pregnancy

. Seizure control should be sought prior to pregnancy. Mephenytoin should be used only after safer anticonvulsants are given an adequate trial and failed. There are no adequate reports or well-controlled studies of mephenytoin in pregnant women. Drug clearance increases between preconception and the 2nd and 3rd trimesters. Thus, many pregnant women require higher doses to maintain therapeutic levels. Mephenytoin is no longer available in the US or the UK. It is still studied largely because of its interesting hydroxylation polymorphism.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether mephenytoin crosses the human placenta. The great majority of mothers on anticonvulsant medication deliver normal infants. Rodent studies suggest that the other hydantoins may not have the same behavioral and teratogenic effects as phenytoin. 648

Breastfeeding

There is no published experience in nursing women. It is unknown whether mephenytoin enters human breast milk.

Pregnancy

. Seizure control should be sought prior to pregnancy. There are no adequate reports or well-controlled studies of mephobarbital in pregnant women. Clearance is altered by

Pregnancy

and may require frequent adjustment through the puerperium. Mephobarbital must be increased in 85% of pregnancies to maintain therapeutic levels. Barbiturates are hepatic enzyme inducers and alter the clearance of many other drugs.

Fetal Health

There are no adequate reports or well-controlled studies of mephobarbital in human fetuses. Barbiturates rapidly cross the human placenta, reaching F:M ratios approaching unity. Retrospective case-control studies suggested a connection between the maternal consumption of barbiturates and a higher than expected incidence of fetal abnormalities. The great majority of women on anticonvulsant medication deliver normal infants. Rodent teratogenicity studies have not apparently been conducted with mephobarbital. 649

Breastfeeding

There is no published experience in nursing women. It is unknown whether mephobarbital enters human breast milk. Small amounts of other barbiturates are excreted.

Pregnancy

. There are no adequate reports or well-controlled studies of meprobamate in pregnant women. Meprobamate decreases clearance of alcohol in rodents during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Meprobamate crosses the human placenta. Several studies suggest an increased prevalence of malformations associated with the 1st trimester use of minor tranquilizers such as meprobamate, chlordiazepoxide, and diazepam. However, there was no clear evidence of either teratogenicity or fetotoxicity following attempted maternal suicide with very large doses. Monotherapy and the lowest effective quantity given in divided doses to minimize the peaks might minimize the risks. While rodent studies reveal that meprobamate reduces the learning ability of mature rodent offspring, this effect is not seen in humans.

Breastfeeding

The small amount of meprobamate entering breast milk and ingested by the nursing newborn (?4% of the weight-adjusted maternal dose) does not pose a clinically significant risk.

Pregnancy

. Mercaptopurine and azathioprine are the most commonly used immunomodulatory agents most commonly encountered during

Pregnancy

in women with inflammatory bowel disease. Both drugs require caution. In addition to the listed indications, mercaptopurine is used as an adjunct to prevent organ rejection after transplantation. There are no adequate reports or well- controlled studies of mercaptopurine in pregnant women. Inflammatory bowel disease can be challenging. Women with quiescent disease are likely to have an uncomplicated pregnancy, whereas those with active disease are more likely to suffer spontaneous abortion, stillbirth, IUGR, and exacerbation of disease. In women considering pregnancy, an active episode should be treated aggressively and remission accomplished before 652

Pregnancy

is attempted. A woman who unexpectedly conceives while her disease is active should be treated aggressively, as remission provides the greatest hope for a favorable outcome. The treatment of AML typically involves a complex drug regimen that includes mercaptopurine. Multiple case reports suggest the use of mercaptopurine can produce a complete and sustained remission culminating in the delivery of a normally developed infant.

Fetal Health

There are no adequate reports or well-controlled studies of mercaptopurine in human fetuses. It likely crosses the human placenta as transient but severe neonatal bone marrow hypoplasia is reported. The impact of mercaptopurine use during the 1st trimester on development is controversial. Retrospective studies conclude there is no increased prevalence of anomalies. However, a more recent population-based cohort study concluded the risk of malformation is increased more than 6-fold. In a second recent report, the incidence of fetal loss was higher in women with inflammatory bowel disease previously treated with mercaptopurine compared to those who had not been so treated. Whether this was related to their older age at conception, longer duration of disease, initially more severe disease, or use of mercaptopurine could not be determined. Although it was suggested mercaptopurine increases the risk of spontaneous abortion, it proved a poor abortifacient in one prospective trial. Exposure during the 2nd and 3rd trimesters does affect the fetal immune system, and birth weight may be reduced. Toxic effects on the neonatal pancreas, liver, and lymphocytes are reported. Rodent studies reveal teratogenicity perhaps mediated by DNA modification or drug-induced changes in mineral metabolism (zinc). Malformations include cleft palate, micrognathia and agnathia, microglossia, short limbs, and gut herniation. Zinc supplementation reduces the risk of an adverse effect.

Breastfeeding

There is no published experience in nursing women. It is unknown whether mercaptopurine enters human breast milk. Until such data become available, it is perhaps best to avoid immunosuppressive medications while breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of meropenem in pregnant women. One multicenter study concluded meropenem is an effective and safe alternative to clindamycin-gentamicin for the treatment of women with acute obstetric infections. There is a case report of its successful use to treat pyogenic sacroiliitis in pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Meropenem crosses the isolated perfused human placenta cotyledon. The mean F:M ratio is 0.04. Maternal and fetal mean meropenem peak concentrations are 54.3 ? 3.3 mcg/ ml and 2.2 ? 0.18 mcg/ml, respectively, and mean trough concentrations are 12.7 ? 1.3 mcg/ml and 0.41 ? 0.10 mcg/ml, respectively. This makes it a poor candidate for fetal treatment. Rodent and monkey studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether meropenem enters human breast milk.

Pregnancy

. Inflammatory bowel disease can be challenging. Women with quiescent disease are likely to have an uncomplicated pregnancy, whereas those with active disease are more likely to suffer spontaneous abortion, stillbirth, IUGR, and exacerbation of disease. This is truer for patients with Crohn?s disease than those with ulcerative colitis. In women considering pregnancy, an active episode should be treated aggressively and remission accomplished before

Pregnancy

is attempted. A woman who unexpectedly conceives while her disease is active should be treated aggressively, as remission provides the greatest hope for a favorable outcome. Mesalamine is a by-product of 5- aminosalicylic acid bound to sulfapyridine. Most patients with adverse effects from sulfasalazine will tolerate mesalamine. Mesalamine is at least equivalent or superior to sulfasalazine, and superior to placebo, with a dose-response benefit, in inducing remission of acute inflammatory bowel disease. It is also comparable to sulfasalazine and superior to placebo for long- term maintenance of remission.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. While it is unknown whether mesalamine crosses the human placenta, only trace amounts of the active metabolite, 5-aminosalicylic acid, can be found in the fetus. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Perhaps the greatest threat to a normal conception is active disease. 656 Inflammatory bowel disease is associated with increased prematurity and decreased birth weight (?330g, adjusted 95% CI: ?509 to ?150g, p <.001); the birth weight is even lower if mesalamine or steroids are required.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. While it is unknown whether mesalamine enters human breast milk, only trace amounts of its active metabolite, 5-aminosalicylic acid, are excreted.

Pregnancy

. Because of its proarrhythmic effect, mesoridazine is indicated for the management of schizophrenic patients who first fail to 657 respond adequately to other antipsychotic drugs. There are no adequate reports or well-controlled studies of mesoridazine in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether mesoridazine crosses the human placenta. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether mesoridazine enters human breast milk.

Pregnancy

. Mestranol is the 3-methyl ether of ethinyl estradiol. An inactive prodrug, it was the estrogen used in many of the first oral contraceptives, and is the estrogen in several currently popular oral contraceptives. Mestranol is demethylated in the liver with a conversion efficiency of 70% (50mcg of mestranol is pharmacokinetically bioequivalent to 35mcg of ethinyl estradiol). The use of oral contraceptives containing mestranol is causally related to an increased incidence of benign liver adenomas and a decreased incidence of benign breast disease. These adenomas are not necessarily worsened by pregnancy. There is sufficient evidence in experimental animals to conclude mestranol is a potential carcinogen. Other estrogens are implicated as human carcinogens. It is now well recognized that there are differences in the physiologic responses to native and synthetic estrogens. There is no indication for mestranol during

Pregnancy

and lactation.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. The observation that maternal administration of mestranol inhibits testosterone synthesis in the rodent fetal testes suggests it crosses the rodent placenta. Limited rodent studies are otherwise reassuring, revealing no evidence of teratogenicity after early

Pregnancy

exposure.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Mestranol enters human breast milk, though the kinetics remain to be detailed. Lactation and infant weight gain are reduced when mestranol is given during the immediate postpartum period. As a result, it is generally considered incompatible with Breastfeeding until the milk reflex is well established.

Pregnancy

. Metaproterenol is a bronchodilator popular during

Pregnancy

for the treatment of asthma. Similar to other b-mimetic agents, metaproterenol increases pulse, lowers BP, and alters the ECG pattern. There are no adequate reports or well-controlled studies of metaproterenol in pregnant women. It has been used as a tocolytic agent (a.k.a. fenoterol, partusisten), but there is no evidence it provides any unique advantage. In vitro, b2-adrenergic agonists are equally potent in inhibiting myometrial contractility as nitroglycerin. There are only case reports of its use during

Pregnancy

in asthmatic women requiring ICU admission. Metaproterenol-saline solution irrigation is used for bronchoalveolar lavage to facilitate restoration of bronchial function.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. While it is unknown whether metaproterenol crosses the human placenta, other b-mimetic agents do. In rabbits, metaproterenol is a teratogen given at doses more than 50the MRHD; there is no adverse effect on other rodents. Studies in animals and humans reveal no evidence that b2-adrenergic agonists pose a CV risk for the fetus and neonate. It may be that b2-adrenoreceptor ontogenesis is completed near term.

Breastfeeding

There is no published experience in nursing women. It is unknown whether metaproterenol enters human breast milk.

Pregnancy

. Metaraminol is a potent sympathomimetic that increases both systolic and diastolic BP. There are no adequate reports or well-controlled studies of metaraminol in pregnant women. Metaraminol has been used to maintain arterial pressure during spinal anesthesia before cesarean delivery, and for CV support in women with septic shock. In vitro, metaraminol is a more potent constrictor of the uterine arteries than ephedrine. The effect is more pronounced in uterine compared to femoral arteries. For that reason, many prefer ephedrine prior to spinal anesthesia. However, a recent RCT suggests metaraminol given as a continuous infusion provides a superior clinical result compared to a continuous infusion of ephedrine. Confirmation of this study would be helpful.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether metaraminol crosses the human placenta. Rodent teratogenicity studies have not been performed. Fetal bradycardia or late decelerations are well- recognized complications of untreated spinal/epidural analgesia? induced hypotension. They are a product of hypotension secondary to peripheral sympathetic blockade. In studies of spinal anesthesia, metaraminol-treated pregnancies may have a lower incidence of neonatal acidosis compared to ephedrine.

Breastfeeding

There is no published experience in nursing women. It is unknown whether metaraminol enters human breast milk. 661 However, considering the dose and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. There is no published experience with metaxalone during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether metaxalone crosses the human placenta. Rodent teratogenicity studies have not been performed. Post-marketing surveys do not suggest any increase in adverse fetal outcomes.

Breastfeeding

There is no published experience in nursing women. It is unknown whether metaxalone enters human breast milk.

Pregnancy

. Metformin is an insulin-sensitizing agent effective in women with PCOS who have significant insulin resistance. PCOS is one of the most common endocrinopathies with approximately 5% of women being affected. Seventy percent of those women taking only metformin and who ovulate conceive in less than 6mo. Metformin also improves the outcome of in vitro fertilization in women with clomiphene-resistant PCOS. There are no adequate 663 reports or well-controlled studies of metformin in pregnant women. Metformin therapy in women with PCOS is associated with a decreased rate of spontaneous abortions and an approximately 10-fold reduction in the incidence of gestational diabetes in case control studies. Metformin and glyburide are proposed as alternatives to insulin in controlling gestational diabetes. Their use remains exciting but investigational.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses, though there is at least one RCT underway. Metformin crosses the isolated, perfused human placental cotyledon. The maternal-fetal transport rates for metformin and antipyrine were 10.61 ? 2.85% and 30.98 ? 5.62%, respectively. The clearance index, calculated as the ratio between the permeabilities of metformin and antipyrine, was 0.34 ? 0.05. It does not block placental glucose uptake and transport in the isolated perfused cotyledon model. In limited clinical study, metformin was not teratogenic, and did not adversely affect birth weight, height, weight, or motor and social development at 3 and 6mo of life. Newborns of women who had their serum glucose levels controlled by metformin do not develop hypoglycemic episodes more frequently than newborns delivered of women treated by insulin alone. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. There is evidence of poor placental transport in the rat.

Breastfeeding

Only 0.28% of the weight-normalized maternal dose of metformin enters human breast milk. In rodents, the metformin concentration in milk approaches that of the maternal plasma. This is well below the 10% level usually expected for the concentration to have a clinical impact.

Pregnancy

. Methacholine is the b-methyl homolog of ACh and differs primarily in its greater duration and selectivity. It is more slowly hydrolyzed by acetylcholinesterase and is almost totally resistant to nonspecific cholinesterase or pseudocholinesterase inactivation. There are no adequate reports or well-controlled studies of methacholine in pregnant women.

Pregnancy

is associated with an improvement in airway responsiveness in asthmatic women.

Fetal Health

There are no adequate reports or well-controlled studies of methacholine in human fetuses. Rodent teratogenicity studies have not been conducted. Based on its physiologic actions, it is unlikely limited exposure to methacholine during a diagnostic procedure would pose a significant risk to the fetus.

Breastfeeding

There is no published experience in nursing women. It is unknown whether methacholine enters human breast milk. However, considering the dose and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. Methadone is a synthetic narcotic analgesic with many actions quantitatively similar to morphine except its intense euphoria. Methadone is a first-line agent for the treatment of heroin addiction. The goal of maintenance is to relieve the narcotic craving, suppress withdrawal, and block the euphoric effects associated with heroin. The majority of patients require 80- 120mg/d or more. Treatment continues for an indefinite period of time. Illicit drug use during

Pregnancy

is a major perinatal health issue worldwide. Some 200,000 addicted infants are born each year in the US. Because most drug-addicted women use a variety of illicit agents, the impact of methadone alone is difficult to ascertain. That said, methadone exposure during the entire gestational period is associated with better drug-treatment outcomes (less illicit drug use) but no greater prevalence of severe neonatal abstinence syndrome than women who begin methadone in the 2nd or 3rd trimester. Methadone is nonsedating. A major problem with opiate-addicted women is postoperative pain management. Methadone-maintained women have similar analgesic needs and responses during labor, but require 70% more opiate analgesic after cesarean delivery. It is generally recommended that methadone treatment be continued while short-acting narcotics are given as necessary (preferably on a fixed schedule) to relieve the pain. The elimination rate of methadone is higher and the t/2 lower during pregnancy, perhaps because of a decrease in the fraction absorbed. Methadone is not recommended for obstetric analgesia because its long duration of action increases the probability of neonatal respiratory depression. Patients maintained on this drug react to life problems and stresses with the same symptoms of anxiety as do others. Do not confuse such symptoms with those of withdrawal and try to treat anxiety by increasing the dose of methadone. The action of methadone in maintenance treatment is limited to the control of narcotic withdrawal symptoms and is ineffective for relief of general anxiety. Maintenance patients on a stable dose of methadone who experience physical trauma, postoperative pain, or other acute pain will not derive analgesia from their ongoing dose of methadone. Instead, they should be administered analgesics, including opioids, in doses that would otherwise be indicated for non?methadone- treated patients with similar painful conditions. Due to the opioid tolerance induced by methadone, somewhat higher and/or more frequent doses will often be required than would be the case for nontolerant patients when opioids are required.

Fetal Health

Methadone crosses the human placenta; however, transfer in the fetal-to-maternal direction is 10-15% greater than in the maternal-to-fetal direction, suggesting involvement of P-glycoprotein. Daily maternal maintenance treatment reduces fetal breathing and total fetal activity. Trough mean plasma methadone concentrations decline as gestation progresses from 0.12mg/L in the 1st trimester to 0.07mg/L in the 3rd trimester. The weight-adjusted clearance rates gradually increase from a mean of 0.17 to 0.21L/hr/kg during pregnancy, although patterns differed substantially among women. Women (and rodents) who continue heroin use throughout

Pregnancy

have a greater likelihood of preterm birth and IUGR. Infants whose mothers are on methadone maintenance have higher mean birth weights and head circumferences than those of untreated addicted women. 667 It is not associated with respiratory depression. However, the withdrawal is more intense in the methadone-treated group compared to heroin-exposed babies without methadone treatment (convulsions 47.1% vs. 27.1%). Maternal methadone dosage is related to the duration of neonatal hospitalization, neonatal abstinence score, and treatment for withdrawal. Interestingly, neonates who undergo withdrawal have almost undetectable concentrations of methadone in their umbilical cord blood. Heroin supplementation does not alter this dose-response relationship. In one study of selected pregnancies, lowering the maternal methadone dose was associated with both a decreased incidence and severity of neonatal withdrawal. Other case-control study conclude that the maternal methadone level does not correlate with neonatal withdrawal. If true, the maternal benefits of effective methadone dosing would not be offset by neonatal harm. Methadone does not appear detrimental for fetal brain development. Some reports suggest an increased incidence of SIDS in neonates delivered of mothers who use methadone during pregnancy. This association may be more circumstantial.

Breastfeeding

Only small quantities of methadone are excreted into human breast milk. It is estimated the average newborn would ingest only 0.05mg methadone per day, an amount too small to reliably prevent neonatal withdrawal. The risk of an adverse event with either Breastfeeding or weaning is low. Newborns of narcotics abusers are at risk for withdrawal despite being breastfed by their methadone-using mother. Pregnant women on methadone maintenance therapy are to be encouraged to nurse if they are HIV-negative.

Pregnancy

. Methamphetamine is a CNS stimulant that has no medical indications during pregnancy. The illicit use of methamphetamine, also called crystal meth or speed, is a major health care problem in some locales. It may be injected, smoked, snorted, or ingested orally. Prolonged use leads to dependence. Five-10% of adolescents have tried methamphetamine and its use is associated with risky sexual behaviors. The use of a variant, Ecstasy (3,4-methylenedioxymethamphetamine) is also becoming more common during pregnancy. Maternal death occurs with usage. Ecstasy users during

Pregnancy

tend to be young and single, report psychological morbidity, and have a higher rate of unplanned pregnancies and a higher likelihood of using other 670 potentially harmful substances (smoking, heavy alcohol intake, and polydrug usage).

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Methamphetamine crosses the human placenta and produces significant and long-lasting maternal and fetal CV effects, including a decrease in fetal PaO2after maternal administration. The latter reflects decreased uteroplacental perfusion, whereas the observed changes in fetal BP and fetal pH are a direct result of methamphetamine. Children of abusers are at risk for IUGR and preterm birth. Antenatal methamphetamine exposure is associated with postnatal developmental disorders associated with neuronal damage, enduring cognitive deficits, and greater risks of neglect and abuse postnatally. Children exposed to methamphetamine antenatally have smaller subcortical volumes and associated neurocognitive deficits compared with a control group. These changes are also associated with abnormalities of brain energy metabolism. The neuronal damage may be mediated by free radical formation, affect the serotoninergic and MAO systems, and differ by fetal gender. Rodent studies reveal embryotoxicity and an increased incidence of microcephaly, NTDs, incomplete rotation of the body axis, and a tortuous spinal cord. Increased frequencies of clefting, cardiac anomalies, and IUGR are reported in humans. Reliable and sensitive screening procedures are available using meconium or hair to identify antenatal exposure to illicit drugs.

Breastfeeding

There is no published experience in nursing women. It is unknown whether methamphetamine enters human breast milk.

Pregnancy

. There is one old report of the use of methantheline to treat N/V of pregnancy.

Fetal Health

There are no published studies in human fetuses. It is unknown whether methantheline crosses the human placenta. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether methantheline enters human breast milk. 672

Pregnancy

. There is no published experience with methazolamide during pregnancy. It is well absorbed orally.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether methazolamide crosses the human placenta. Methazolamide causes skeletal abnormalities in rodents when given at high multiples of the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether methazolamide enters human breast milk. 673

Pregnancy

. There are no adequate reports or well-controlled studies of methenamine in pregnant women. Methenamine is used for chronic suppressive treatment of bacteriuria during pregnancy. Approximately 80% of the oral dose is excreted into the urine within 24h. Pathogens resistant to other antibacterial agents may respond to methenamine because of the nonspecific effect of formaldehyde formed in the acid urine.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Methenamine crosses the human placenta. The concentration of methenamine in umbilical cord plasma is low, approximating that in maternal plasma after 4h. Low concentrations of methenamine are also found in amniotic fluid. Rodent teratogenicity studies have not been conducted.

Breastfeeding

Methenamine enters human breast milk at a concentration similar to maternal plasma. It is generally considered compatible with breastfeeding. 674

Pregnancy

. The role of methicillin in therapy has been largely replaced by flucloxacillin and dicloxacillin. However, the phrase ??methicillin- resistant Staphylococcus aureus?? continues to be used to describe S. aureus strains resistant to all penicillins. Pregnant women often have mixed vaginal flora of both MSSA and MRSA. Strains of MRSA are a major cause of nosocomial infection. Chorioamnionitis with MRSA is a rare complication of pregnancy. There are no adequate reports or well-controlled studies of methicillin in pregnant women. Epidemiological studies suggest colonization rates in

Pregnancy

reflect the local populace.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Methicillin crosses the human placenta, achieving an M:F ratio approximating unity. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Routine surveillance reveals a rising incidence of MRSA infections in NICUs. Maternal-neonatal transmission of MRSA is documented.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Methicillin enters human breast milk, though the kinetics remain to be elucidated. There is only limited published experience in women with mastitis; most cases are secondary to methicillin-sensitive staphylococci. Mastitis secondary to MRSA is reported, as is toxic shock syndrome. Methicillin is generally considered compatible for Breastfeeding based on this clinical experience. 675

Pregnancy

. Several clinical aspects of hyperthyroidism have received special attention in the recent past. Hyperthyroidism associated with hyperemesis gravidarium was originally believed secondary to 676 inappropriate secretion of b-hCG. More recently, a mutation in the thyrotropin-releasing hormone receptor was discovered. It does not require treatment. The most common cause of maternal hyperthyroidism during

Pregnancy

is Graves? disease. The mainstay of treatment is an antithyroid drug, either propylthiouracil or methimazole. During a 12w study of Graves? hyperthyroidism, a single daily dose of 15mg methimazole was much more effective in the induction of euthyroidism than a single daily dose of 150mg propylthiouracil. Thyroid function tests should be obtained during gestation in women suffering from hyperthyroidism and the dose of methimazole adjusted accordingly to keep T3and T4within the upper normal range for these women. The lowest effective dose is recommended. Women previously treated with either a radioactive cocktail or thyroidectomy may still be producing thyroid-stimulating immunoglobulin even though they are themselves euthyroid. If the level is elevated, the fetus is at risk and should be referred to a fetal center for evaluation (see Propylthiouracil).

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Methimazole crosses the human placenta and is an alternative to propylthiouracil for the treatment of fetal hyperthyroidism secondary to thyroid-stimulating immunoglobulin. The fetal response is often different than the maternal, and some recommend it be tested directly. Methimazole can induce fetal goiter and even cretinism in a dose-dependent fashion. Recent studies of exposed children followed until 3-11y reveal no deleterious effects on either thyroid function or physical and intellectual development with doses up to 20mg daily. However, rare instances of aplasia cutis (manifest as scalp defects), esophageal atresia with tracheoesophageal fistula, and choanal atresia with absent/hypoplastic nipples (methimazole syndrome) are reported, suggesting methimazole may be a weak human teratogen. More recent studies have been unable to confirm a significant teratogenic difference between methimazole and propylthiouracil.

Breastfeeding

Methimazole is excreted in human breast milk, but the quantities are small (2-3%) and neonatal thyroid function unaltered. Several recent studies observed no deleterious effects on neonatal thyroid function or on physical and intellectual development of breastfed infants whose mothers were treated with up to 20mg daily.

Pregnancy

. There is no published experience during pregnancy. Methocarbamol has no direct effect on the contractile mechanism of striated muscle, the motor end plate or the nerve fiber.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether methocarbamol crosses the human placenta. Rodent teratogen studies have not been performed. 678

Breastfeeding

There is no published experience with methocarbamol in nursing women. The manufacturer indicates minimal amounts are found in the milk, though no details are provided.

Pregnancy

. Methohexital is an ultra-short-acting barbiturate. Compared with thiamylal and thiopental, methohexital is at least twice as potent on a weight basis and lasts only half as long. Cumulative effects are fewer and recovery is more rapid than with thiobarbiturates. When used for cesarean delivery, analgesic requirements during the 1st postoperative hour are increased compared to propofol. It appears similar to propofol when used for 1st trimester suction abortion in terms of efficacy, acceptability, cost, and Side effects include arrhythmias, tachycardia, bradycardia, CV collapse, hypotension, dyspnea, respiratory depression, excitatory phenomena, and thrombophlebitis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Methohexital rapidly crosses the placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically (6-7the MRHD). Breastfeeding There is no published experience in nursing women. It is unknown whether methohexital enters human breast milk. 679 Considering its rapid clearance, it is unlikely a clinically significant amount would enter the breast milk when used for the noted indications.

Pregnancy

. Methotrexate is an antimetabolite with multiple uses in reproductive-age women, including the treatment of ectopic pregnancy, neoplastic disease, autoimmune disorders, and inflammatory conditions. Methotrexate originated in the 1940s when Dr. Sidney Farber at Children?s Hospital Boston was testing the effects of folic acid on acute childhood leukemia. Inspired, he asked Lederle Laboratories to synthesize methotrexate. Dr. Farber then administered it to a small group of very ill children. The remarkable clinical improvement he observed began the era of modern cancer chemotherapy. Ectopic pregnancy: Ectopic

Pregnancy

is a major cause of maternal morbidity and mortality. Its treatment remains primarily surgical, but medical treatment is routine in some locales. Criteria include serum b-hCG titer <5000IU/L, at most free fluid confined to the pelvis, and

Pregnancy

diameter <3.5cm. Surgery is preferred after tubal rupture, or with a high potential for rupture, hypotension, and anemia, or a

Pregnancy

>3.5cm diameter. Some report that methotrexate is safe and effective for the treatment of a hemodynamically stable ectopic characterized by an adnexal mass up to 5cm, or a b-hCG titer >5000IU/L. Larger trials are needed for confirmation. Treatment often leads to an increase in mass size and should not be considered a sign of failure. Severe abdominal/pelvic pain may follow, and the surgeon must determine whether the pain is secondary to medical treatment or failure of the methotrexate and rupture of the ectopic. Persistent ectopic

Pregnancy

is usually diagnosed when there is abdominal pain, intra-abdominal hemorrhage, or plateau b-hCG titers. In those situations, methotrexate can be administered a 2nd time. Ten to 20% of treated women ultimately require surgery. Methotrexate does not alter subsequent ovarian reserve. Though the greatest experience is with a tubal ectopic, there are case reports supporting its use in cervical, corneal, interstitial, and uterine incision scar ectopic pregnancies. Oral methotrexate (60mg/m2) may also be successful, though the body of clinical experience is small. Local injection of methotrexate reduces the frequency of persistent ectopic

Pregnancy

after linear salpingostomy. GTD: Methotrexate is a first choice for uncomplicated malignant trophoblastic disease. Resistance to methotrexate is encountered requiring the use of alternative drug regimens (see melphalan). Prognostic factors useful for treatment decisions divide women into low-, medium-, and high-risk groups. Low-risk patients are treated by a single agent, preferably methotrexate. Medium- to high-risk populations require multidrug regimens that frequently include methotrexate. Women should avoid

Pregnancy

until their b-hCG titer is normal for 1y. Medical abortion: Methotrexate has been used to induce a medical abortion of an intrauterine pregnancy. It is more effective combined with misoprostol than alone. As it is not 100% effective, women must be followed clinically until there is complete normalization of b-hCG titers from their serum.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether methotrexate crosses the human placenta. Methotrexate is rapidly taken up by the trophoblast in a fashion that does not interfere with folate uptake, and then extruded. It seems reasonable to conclude that 1st trimester exposure results in an increased risk of internal and external malformations (craniofacial, axial skeletal, cardiopulmonary, GI and dermatologic abnormalities) and developmental delay, though most pregnancies exposed to low doses are successful. The teratogenic effect is enhanced by the addition of misoprostil. Others report no association between later

Pregnancy

exposure and congenital abnormalities.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether methotrexate enters human breast milk. Despite the lack of information, methotrexate is generally considered contraindicated in nursing mothers.

Pregnancy

. Methotrimeprazine is an aliphatic phenothiazine neuroleptic drug that produces sedation and tranquilization (also called levomepromazine). There are no adequate reports or well- controlled studies of methotrimeprazine in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether methotrimeprazine crosses the human placenta. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether methotrimeprazine enters human breast milk.

Pregnancy

. Neuraxial analgesia is frequently accompanied by hypotension. If untreated, there are many well-described maternal and fetal effects. Perioperative hypotension may be controlled by methoxamine should ephedrine fail. There are no adequate reports or well-controlled studies of methoxamine in pregnant women. It decreases uterine blood flow in pregnant ewes and monkeys at doses similar to human. In rats, methoxamine increases uterine contractility in a dose-dependent fashion. It is unclear whether the same occurs in humans. Methoxamine was used in one study to alter afterload as part of an evaluation of women thought recovered from peripartal cardiomyopathy. If used to correct hypotension during labor and delivery, oxytocic drugs such as ergonovine, ergotamine, methylergonovine, and vasopressin may cause severe hypertension.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether methoxamine crosses the human placenta. It decreases uterine blood flow and, consequently, causes fetal bradycardia and acidemia when given to pregnant ewes and monkeys at doses similar to human doses. Doppler studies reveal a brief increase in uterine artery pulsatility index after methoxamine for epidural-related hypotension, whereas ephedrine has no effect. This short-lived effect is small compared to the effect of the hypotension. 685

Breastfeeding

There is no published experience in nursing women. It is unknown whether methoxamine enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of methoxsalen in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether methoxsalen crosses the human placenta. Rodent teratogenicity studies have not been performed. In one limited study, there was no increase in the risk of specific defects after exposure to methoxsalen, but it may be embryotoxic.

Breastfeeding

There is no published experience in nursing women. It is unknown whether methoxsalen enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of methscopolamine in pregnant women. It can also be used for stomach or intestinal spasms, to reduce salivation, and to treat motion sickness. Methscopolamine is also commonly used as a drying agent in cold and allergy medications (Extendryl, AlleRx, Rescon). (See Scopolamine.) 687

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether methscopolamine crosses the human placenta. Rodent teratogenicity studies have not been performed. (See Scopolamine.)

Breastfeeding

There is no published experience in nursing women. It is unknown whether methscopolamine enters human breast milk. (See Scopolamine.)

Pregnancy

. Methsuximide is indicated for the control of absence (petit mal) seizures refractory to other drugs. There is no published experience during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether methsuximide crosses the human placenta. Rodent teratogenicity studies have not been conducted. Many anticonvulsants are associated with an increased risk of malformation. The limited experience with methsuximide precludes comment. As for most anticonvulsant drugs, using 688 monotherapy and the lowest effective quantity given in divided doses to minimize the peaks can minimize the risks.

Breastfeeding

There is no published experience in nursing women. It is unknown whether methsuximide enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of methyclothiazide in pregnant women. Thiazides and other diuretics are inappropriate treatment for physiologic edema of pregnancy. They are not indicated for the treatment of preeclampsia. (See Chlorothiazide.)

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether methyclothiazide crosses the human placenta. Other thiazide diuretics do cross. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. (See Chlorothiazide.)

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether methyclothiazide enters 689 human breast milk. Other thiazide diuretics are excreted into milk. (See Chlorothiazide.)

Pregnancy

. There are no adequate reports or well-controlled studies of methylcellulose in pregnant women. Methylcellulose is frequently used in the gel preparations for local application of prostaglandin or relaxin. Like cellulose, it is neither digestible, toxic, nor allergenic. Systemic absorption is likely low.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Based on molecular size, it is unlikely methylcellulose crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Methylcellulose did not influence behavior, appearance, or growth postnatally.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether methylcellulose enters human breast milk. Animal studies reveal no evidence that methylcellulose adversely affects lactation. 690

Pregnancy

. One to 6% of young women have chronic hypertension. Methyldopa is perhaps the best-studied antihypertensive agent during pregnancy. It remains a first-line agent for the treatment of moderate to mild hypertension. Methyldopa requires 48-72h to exert its effect. The delay can be reduced to <12h if the patient is loaded either parenterally or orally. Hypertension predating

Pregnancy

should be differentiated from preeclampsia. While treatment is indicated for women with a systolic BP >170mmHg and/or a diastolic BP >109mmHg, there is no consensus whether lesser degrees of hypertension require treatment during pregnancy. In women with mild to moderate chronic hypertension, antihypertensive therapy improves the 691 maternal but apparently not the fetal outcome. In such patients, methyldopa prolongs

Pregnancy

by some 10d compared to placebo, but does not decrease the prevalence of superimposed preeclampsia. Methyldopa is less effective than metoprolol, but as effective as nifedipine, labetalol, and ketanserin, in decreasing both systolic and diastolic BP in women with chronic hypertension. On average, methyldopa decreases the maternal MAP 10.0mmHg and the mean heart rate by 6.0 bpm. The hypotensive effect is associated with a decrease in sFH-1 and an increase in PIGF. The uterine artery pulsatility index is generally unchanged. One small cohort study of early antihypertensive treatment with methyldopa in normotensive pregnant women with type 1 diabetes and microalbuminuria observed a significant reduction in preterm birth <34w. This finding needs prospective confirmation. Neither short- nor long-term use of methyldopa is associated with adverse maternal effects. Rare, sporadic cases of reactive hepatitis are reported in women treated with methyldopa during pregnancy. In chronically hypertensive women, methyldopa increases prolactin, thyrotropin, and T3in a dose-dependent fashion, indicating decreased dopaminergic inhibition of pituitary hormone release. In contrast, methyldopa decreases plasma T4levels.

Fetal Health

Most antihypertensive agents cross the placental barrier. Methyldopa is the only drug accepted for use during the 1st trimester of pregnancy. Neither short- nor long-term effects on the fetus or the neonate are reported after long-term methyldopa use. Methyldopa does not significantly alter fetal cardiac activity or produce any fetal hemodynamic changes as measured by Doppler flow studies. In contrast, methyldopa decreases placental vascular resistance in mild preeclampsia and in chronic hypertension. The available data are inadequate to conclude whether methyldopa adversely affects the fetal or neonatal HR and pattern. Until such data are available, FHR changes cannot be reliably attributed to drug effect, but rather may be due to progression of the underlying maternal or placental disease. Longitudinal studies revealed no developmental disturbances at 3y in children exposed in utero. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Methyldopa enters human breast milk, but the M:P ratio is low. Breastfed neonates delivered of women who are using methyldopa are normotensive.

Pregnancy

. Methylene blue causes smooth muscle contraction of many vessels, including the uterine arteries, by inhibiting guanylate cyclase. In the past, methylene blue was injected intra-amniotically to facilitate the diagnosis of PPROM and to demonstrate that independent sacs were sampled during amniocentesis of a multiple gestation. Based on concerns of vasoconstriction and case reports of methemoglobinemia in susceptible women, methylene blue has been largely replaced by indigo carmine for amniocentesis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Methylene blue crosses the human placenta after intra-amniotic injection and is excreted in the maternal urine. Preterm neonates with G6PD deficiency exposed in utero may experience severe hemolysis and hyperbilirubinemia requiring exchange transfusion. A specific syndrome is described that includes hemolytic anemia, hyperbilirubinemia, and methemoglobinemia. Photosensitization is reported in very-low- birth-weight neonates exposed prenatally. Methylene blue use for 2nd trimester amniocentesis in twin gestation is associated with a dose-dependent increased risk of fetal intestinal atresia and/or death. In rodents, methylene blue given late in gestation induces preterm delivery and IUGR.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether methylene blue enters human breast milk. It is excreted into the milk of cows and goats.

Pregnancy

. Postpartum hemorrhage remains a leading cause of maternal death and morbidity. Oxytocin, methylergonovine, and several prostaglandin agents are the pharmacologic agents most frequently used to prevent or treat postpartum hemorrhage. There is a long clinical experience with methylergonovine. It is effective and inexpensive. Unfortunately, its shelf life is compromised in tropical climates, where misoprostol may be preferable. Methylergonovine is typically administered in the immediate postpartum period when oxytocin alone fails to control myometrial atony. However, it is not effective prophylaxis for atony after delivery, and its administration with delivery of the anterior shoulder may actually increase the risk of a retained placenta. One RCT concluded oxytocin after delivery of the anterior shoulder was superior to methylergonovine administered after delivery of the placenta for the prevention of postpartum hemorrhage. The half-life of methylergonovine is 1-3min, its onset of action 2-5min after IM and 5-10min after oral administration. IM is more effective than PO for the treatment of atony; the IV route is usually avoided unless the dose is diluted and infused slowly due to potential hypertension (perhaps causing stroke or MI) or vascular/tissue damage due to extravasation. There are potential interactions of methylergonovine and vasoactive agents, which perhaps have been administered to treat hemorrhagic hypotension. Therefore, there must be communication between the obstetrician and anesthesiologist at an operative delivery with unexpected blood loss before the methylergonovine is given. The combination of oxytocin and methylergonovine is more effective than oxytocin and misoprostol with fewer Side effects include MI, N/V, diarrhea, headache, hallucinations, hypertension, chest pain, tinnitus, nasal congestion, hematuria, dyspnea, thrombophlebitis, and dizziness.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether methylergonovine crosses 695 the human placenta. Rodent teratogenicity studies have not been performed. Inadvertent administration during

Pregnancy

is followed by tetanic contractions and fetal bradycardia. Breastfeeding There are no adequate reports or well-controlled studies in nursing women. The concentrations of methylergonovine in human breast milk are clinically insignificant. While some reports suggest methylergonovine may decrease milk production, it has been used for decades PO tid or qid up to 1w to prevent postpartum hemorrhage without adverse effects on either lactation or the newborn.

Pregnancy

. There are no adequate reports or well-controlled studies of methylphenidate in pregnant women. The clinical experience consists of limited case reports of narcolepsy and substance abuse.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether methylphenidate crosses the human placenta, and limited human data do not indicate a significant risk of structural abnormalities. However, maternal abuse of pentazocine and methylphenidate is associated with preterm birth, IUGR, and evidence of neonatal withdrawal. Rodent teratogenicity studies reveal skeletal abnormalities in rabbits treated with 40the MRHD. IUGR was seen in lower doses. Lastly, rodent studies suggest a possible impact on brain development.

Breastfeeding

There is no published experience in nursing women. Methylphenidate enters human breast milk, but the kinetics remain to be detailed. 697

Pregnancy

. Methylprednisolone is effective treatment for a wide range of disorders that occur during pregnancy. The large number prevents a detailed list here. Most synthetic corticosteroids are absorbed rapidly and completely when administered orally and are eliminated by the liver through the action of the enzyme CYP3A4. Smaller amounts are eliminated by the kidney (10-30%). The elimination t/2 is short (e.g., in nonpregnant adults, 2.3 ? 0.5h); however, the biologic activity is much longer (12-36h). Methylprednisolone is effective and believed safe during

Pregnancy

for the treatment of acute asthma, lupus, nephrotic syndrome with mixed connective tissue disease, immune glomerulonephritis, alloimmune thrombocytopenia, immune thrombocytopenia, inflammatory bowel disease, Bell?s palsy, and gestational herpes, and for a ??stress?? dose in labor and delivery to chronically suppressed patients, among many other uses. Other inflammatory disorders such as de Quervain?s disease of

Pregnancy

can be treated successfully. It has been suggested that 1st trimester hyperemesis gravidarium refractory to conventional treatments can be treated with methylprednisolone. However, a recent RCT concluded that the addition of parenteral and oral methylprednisolone to the treatment of women with hyperemesis gravidarum did not reduce the need for rehospitalization later in pregnancy. Steroids may also be useful in reducing the severity and speeding the recovery of women who develop atypical preeclampsia, or HELLP syndrome. Methylprednisolone reduces the risk of ovarian hyperstimulation during ovulation induction for in vitro fertilization.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Methylprednisolone does not cross the placenta. However, a recent RCT concluded that high-dose methylprednisolone reduces fetal exposure to hyperthermia and inflammation, but increases the rate of neonatal asymptomatic bacteremia. Stress-dose corticosteroid use in labor should trigger consideration of a screening neonatal blood culture. Rodent teratogenicity studies have not been performed, but there is no clinical evidence it is teratogenic. The effect of bolus doses of methylprednisolone on the fetus is unknown.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether methylprednisolone enters human breast milk. What little evidence exists suggests the quantity of corticosteroid excreted into breast milk is not clinically relevant for the newborn.

Pregnancy

. Methyltestosterone is used with modest results for the treatment of endometriosis in infertile women. It is used for palliation with advancing inoperable breast cancer known or believed to be estrogen-sensitive. Methyltestosterone is also used in combination with estrogen to enhance libido in women. There are no adequate reports or well-controlled studies of methyltestosterone in pregnant women, nor are there indications for its use.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether methyltestosterone crosses the human placenta. It does increase placental estradiol synthesis in vitro. Animal studies (rodents, dog) reveal pseudohermaphroditism in female fetuses exposed to methyltestosterone.

Breastfeeding

There is no published experience in nursing women. It is unknown whether methyltestosterone enters human breast milk. It is ineffective for suppressing lactation.

Pregnancy

. Methysergide is a semisynthetic, ergot ergometrine alkaloid derivative that constricts cranial and peripheral blood vessels. It is used prophylactically to treat migraine headache. There are no adequate reports or well-controlled studies of methysergide in pregnant women. Despite the limited clinical data to provide guidance, methysergide is generally considered contraindicated during

Pregnancy

because of its vasoconstrictive effects.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether methysergide crosses the human placenta. Rodent studies reveal evidence of embryotoxicity and bradycardia when administered at high doses. It is suspected that the toxic effects are vascularly mediated, and not a direct myocardial effect.

Breastfeeding

There is no published experience in nursing women. It is unknown whether methysergide enters human breast milk.

Pregnancy

. N/V are common during the 1st trimester. Metoclopramide effectively reduces the incidence and severity, but may be associated with an increased risk of preterm delivery. It is unclear whether this relationship is related to metoclopramide or to the underlying disease. The insufficient data on the safety of metoclopramide makes it a second-line agent for the treatment of hyperemesis or gastroesophageal reflux. Metoclopramide is highly effective controlling N/V during surgery in women undergoing cesarean section. It reduces gastric secretions but does not decrease the quantity of narcotics used to control pain postoperatively. In contrast, metoclopramide significantly reduces the duration of labor and the total PCA morphine requirements of women undergoing prostaglandin-induced abortion. To reduce 703 the risk of dystonia, patients may be premedicated with diphenhydramine. Metoclopramide is also helpful for the treatment of migraine, and enhances erythropoiesis in women with Diamond-Blackfan anemia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Metoclopramide crosses the human placenta, though the kinetics remain to be elucidated. Its use in the 1st trimester does not appear to be associated with an increased risk of malformations, spontaneous abortions, or decreased fetal birth weight. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Metoclopramide transfer was examined in 18 women who were 8-12w postpartum. It was detected in all samples, typically with an M:P ratio >1. However, metoclopramide was found in only 1 of the 5 neonates studied. Exposure of the child ranged from 6-24 mcg/kg/day in the early puerperium to 1-13 mcg/kg/day in the late puerperium. These quantities are considerably less than the therapeutic dose of 500 mcg/kg/day recommended for children. Metoclopramide is said to augment milk production without altering the prolactin or sodium concentrations. However, one RCT in women delivered prematurely concluded it does not improve breast milk volume or the duration of breastfeeding.

Pregnancy

. The use of diuretics in an otherwise healthy woman is inappropriate and exposes mother and fetus to unnecessary hazard. Diuretics do not prevent the development of preeclampsia, and there is no evidence that they are useful in the treatment of those with the disease. (See Chlorothiazide.) 705

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether metolazone crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. (See Chlorothiazide.)

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Metolazone enters human breast milk, but the kinetics remain to be elucidated. (See Chlorothiazide.)

Pregnancy

. Metoprolol is effective for the treatment of mild to moderate chronic hypertension, stable angina, arrhythmia, and post-MI patients. Metoprolol was extensively tested during

Pregnancy

and deemed safe. Its clearance is increased during pregnancy, and the dose may require upward revision each trimester. Metoprolol is more effective than methyldopa in decreasing both systolic and diastolic BP in women with chronic hypertension, but less effective than nicardipine. There are many case reports of its use during

Pregnancy

without apparent adverse effects. In principle, the management of an arrhythmia is similar whether the patient is pregnant or not. Metoprolol has been used successfully to correct supraventricular arrhythmias. It may also reduce the frequency of migraine headache during

Pregnancy

when given prophylactically. Metoprolol is as effective as propranolol in controlling symptoms of hyperthyroidism.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Metoprolol crosses the human placenta, but does not adversely affect the FHR. Some studies of b-blockers in

Pregnancy

reveal an increased risk of IUGR. While true with atenolol and propranolol, it is not noted with metoprolol. Current study suggests the cause of IUGR is excessive b blockade, producing a decrease in maternal cardiac output. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. High doses are associated with embryotoxicity.

Breastfeeding

Small quantities of metoprolol are excreted into human breast milk. The neonatal plasma level is either very low or undetectable between Breastfeeding periods. Feeding 3-4h after the maternal dose further reduces the neonatal risk.

Pregnancy

. Metronidazole is used widely during

Pregnancy

and has multiple therapeutic benefits. Bacterial vaginosis: BV is associated with preterm rupture of membrane, preterm labor and delivery, and postpartum endometritis. Systemic and local therapy with metronidazole effectively treats BV. Several large randomized trials seeking to determine whether successful treatment of BV reduced the prevalence of adverse outcomes ended in controversy. Women who deliver preterm with symptomatic BV have a lower risk of preterm birth in a subsequent

Pregnancy

if treated with 709 metronidazole. Unfortunately, the treatment of women with asymptomatic BV and no prior preterm birth apparently does not alter their preterm delivery rate. High-risk conditions that require treatment of BV with metronidazole include women with prior preterm birth, body mass index <19.8kg/m2, and evidence of endometritis before pregnancy. A ??test of cure?? should be obtained 1mo later. Small trials suggest that the combination of ampicillin and metronidazole successfully prolongs

Pregnancy

in women with threatened idiopathic preterm labor. Similar results are reported when metronidazole is combined with erythromycin. Unfortunately, an appropriately sized RCT comparing metronidazole plus ampicillin at 24w and intrapartum had no effect on preterm birth despite reducing the prevalence of BV. In several of the RCTs, women with asymptomatic BV who took metronidazole before 26w gestation actually had a higher incidence of preterm labor than controls. In another RCT focusing on women with a positive cervical fetal fibronectin in the 2nd trimester, metronidazole treatment was associated with a near doubling of the preterm birth rate compared to placebo. BV treatment may offer other benefits. Prophylactic IV metronidazole reduces infectious morbidity postoperatively after a clinically indicated cesarean section. Similar results are obtained when metronidazole is applied PV. Metronidazole also decreases the risk of upper genital tract infection after 1st trimester suction curettage. Trichomoniasis is associated with an increased incidence of adverse outcomes of pregnancy. A single dose of metronidazole cures 90%. The cure rate is higher if both partners are treated. Unfortunately, the treatment of pregnant women with asymptomatic trichomoniasis does not prevent preterm delivery. It is not known whether the result is different for symptomatic disease. Other diseases such as inflammatory bowel disease, C. difficile colitis, and anaerobic and protozoal infections are successfully treated during

Pregnancy

with short-term courses of metronidazole.

Fetal Health

Metronidazole crosses the human placenta. Though achieving an F:M ratio near unity, it does not pose a major teratogenic risk when used in the recommended doses. The safety of drug therapy for inflammatory bowel disease during

Pregnancy

is an important clinical concern. Metronidazole appears safe if used for short durations. The possible fetal adverse effects related with long-term exposure as required by this condition remain unknown. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity occurs.

Breastfeeding

Metronidazole is excreted into human breast milk, reaching an M:P ratio greater than unity, but is not associated with adverse effects in breastfed neonates.

Pregnancy

. Mexiletine is a local anesthetic structurally similar to lidocaine but active orally. There are no adequate reports or well-controlled studies of mexiletine in pregnant women. The published experience during

Pregnancy

is limited to a few case reports where the drug was used throughout gestation to treat symptomatic PVCs. The dose requires monitoring to ensure that therapeutic levels are maintained. Mexiletine has also been used for the treatment of chronic neuropathic pain.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether mexiletine crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Some embryotoxicity was noted at doses that were multiples of the MRHD.

Breastfeeding

Mexiletine is excreted into human breast milk, achieving an M:P ratio greater than unity. However, the neonatal concentration does not reach a clinically relevant level because of the volume of distribution.

Pregnancy

. Mezlocillin, alone or in combination with other antibiotics, is effective as treatment or prophylaxis for a variety of diseases during pregnancy, including pyelonephritis, puerperal endomyometritis, and PPROM, or for cesarean section prophylaxis. In several small trials, mezlocillin prolonged the latency interval after PPROM. Mezlocillin is considered as safe and effective as cefoxitin and clindamycin/gentamicin for treatment of postpartum endometritis. A single perioperative dose of mezlocillin is as effective as a 3-dose regimen of either mezlocillin or cefoxitin in preventing postoperative endometritis after a cesarean section. Because there is no antibiotic that provides superior postcesarean prophylaxis, the decision is usually based on cost.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Mezlocillin crosses the placenta and is found in low concentrations in fetal blood and AF. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Low concentrations of mezlocillin are found in human breast milk, too low to achieve a clinically relevant level in the fetus. Other penicillins are generally considered compatible with breastfeeding.

Pregnancy

. Candida vaginitis is perhaps the most common female genital tract infection. The vaginal milieu during

Pregnancy

predisposes to C. albicans overgrowth. There are no adequate reports or well- controlled studies of miconazole in pregnant women. There is controversy whether the various imidazole compounds differ in efficacy for mycotic vaginitis. Studies conducted immediately after miconazole was released suggested it was significantly better than nystatin, clotrimazole, and butoconazole for the treatment of vaginal candidiasis during gestation. However, no RCT substantiates that conclusion. There is no significant difference in cure rates achieved after 7-14d of therapy. Significantly more patients relapsed after cure in the nystatin and clotrimazole groups than in the miconazole groups. Miconazole is as effective 715 as oral therapy with fluconazole for vulvovaginal candidiasis. About 25-30% of the oral dose, but less than 0.1% of the vaginal dose, is absorbed. Though women frequently prefer oral medication, fluconazole is not recommended during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether miconazole crosses the human placenta, but it has been used successfully in newborns. In vitro, miconazole effectively inhibits placental and fetal adrenal steroid aromatase. Miconazole is absorbed systemically after vaginal application, reaching peak levels approximating 10ng/ml. In contrast, parenteral levels of miconazole exceed mcg/ml. Post- marketing studies are reassuring, revealing no excess rates of adverse outcomes. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity is associated with doses that also produce maternal toxicity.

Breastfeeding

There is no published experience in nursing women. It is unknown whether miconazole enters human breast milk. However, considering the dose and route, it is unlikely the breastfed neonate of a woman being treated for vaginitis with vaginal applications would ingest clinically relevant amounts.

Pregnancy

. Outpatient surgery demands rapid recovery with minimal delay. The short-acting sedation of midazolam makes it one of the most frequently used benzodiazepines for short surgical procedures. It is most appropriate for those who are particularly anxious. Conscious sedation with midazolam and fentanyl significantly improves patient satisfaction with 1st trimester termination performed under local anesthesia. Similar results are obtained in women undergoing outpatient procedures such as oocyte retrieval procedure or GIFT. In one RCT, intrathecal midazolam (2mg) prolonged the postcesarean analgesia when used as an adjunct to bupivacaine. In yet another RCT, intrathecal midazolam increased the analgesic effect of fentanyl without any increase in adverse outcomes. In addition, both the 1 and 2mg doses decreased postoperative N/V. In another double-blind RCT, healthy women received either a combination of 1mcg/kg fentanyl and 0.02mg/kg midazolam IV, or an equal volume of saline IV at the time of their skin preparation for a bupivacaine spinal anesthetic. Fetal outcome measures included Apgar scores, continuous pulse oximetry for 3h, and neurobehavioral scores. Maternal outcomes included catecholamine levels, and recall of anesthesia and delivery. There were no between-group differences of neonatal outcome variables (Apgar score, neurobehavioral scores, continuous oxygen saturation). Mothers in both groups showed no difference in their ability to recall the birth of their babies. Midazolam levels are increased during

Pregnancy

suggesting a decrease in CYP3A4 activity. In rodents, midazolam suppresses uterine contractility in vitro. 717

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Midazolam crosses the human placenta somewhat more slowly than diazepam, achieving an F:M concentration ratio approaching unity 30-60min after maternal injection. Postnatally, its elimination t/2 is 6-7h. The reported effects of benzodiazepines on development are inconsistent. Studies in the 1970s suggested 1st trimester exposure to benzodiazepines increased the risk of facial clefts, cardiac malformations, and other multiple malformations. Yet, no syndrome could be described. Diazepam and chlordiazepoxide were most frequently implicated. However, an increased risk was not confirmed in recent studies. Midazolam use during the 3rd trimester or labor may be associated with floppy infant syndrome, or symptoms of neonatal withdrawal. These symptoms vary among mild sedation, hypotonia, apneic spells, cyanosis, impaired metabolic responses to cold stress, and reluctance to suck, and may persist for hours to months after birth.

Breastfeeding

Midazolam is excreted at low concentrations into human breast milk with an M:P ratio approximating 0.15 and less than 0.05% of the maternal dose in 24h. Considering the dose and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. Midodrine increases vascular tone and elevates BP. In a single case report, midodrine was used successfully to treat postural 719 orthostatic tachycardia syndrome (POTS), a rare disease characterized by syncope, sinus tachycardia, and orthostasis due to autonomic dysfunction. Rodent studies reveal no effect on uterine contractility in vitro.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether midodrine crosses the human placenta. Though no evidence of teratogenicity was found in rodent studies, there was an increased prevalence of embryo resorption and IUGR.

Breastfeeding

There is no published experience in nursing women. It is unknown whether midodrine enters human breast milk.

Pregnancy

. Sheep studies demonstrate that progesterone suppresses uterine/ placental secretion of PGF-2a, and that critical progesterone: estradiol-17b and PGE:PGF-2a ratios are necessary for continuation of the pregnancy. Mifepristone causes progesterone withdrawal. It is a possible emergency contraceptive after unprotected coitus (10mg) effective for up to 6d after exposure. Low-dose mifepristone (either 25mg PO ?1, or 10mg PO ?1 followed by levonorgestrel 1.5mg PO 12h later) is 80% effective. In 1996, the FDA Advisory Committee for Reproductive Health Drugs concluded mifepristone was safe and effective for early

Pregnancy

termination. In 2000, the FDA approved mifepristone to induce abortion in pregnancies <49d from the LMP. The most popular treatment schedule is mifepristone 200-600mg followed 36-48h later by oral misoprostol (0.4-0.6mg) in pregnancies up to 49d, and vaginal gemeprost (1.0mg) or misoprostol (0.8mg) if the

Pregnancy

dates from 49 to 63d since the LMP. The addition of 2 doses of misoprostol beginning 48h after mifepristone significantly reduces the ongoing

Pregnancy

rate compared to mifepristone alone. In another report, a fixed protocol of 200mg of mifepristone PO followed by 0.4mg misoprostol PV 2d later was compared to a flexible dosing interval of 1, 2, or 3d between mifepristone and misoprostol. At the same time, the upper limit of gestational age was increased from 56 to 63 days. The rates of complete abortion were 94.9% and 94.4% (not significant), respectively. Continuing

Pregnancy

was rare (0.7%). b-hCG and progesterone concentrations continue to increase for 48h after mifepristone. After misoprostol, the b-hCG and progesterone levels decline in 24h by 70% and 60%, respectively. Treated women should expect some bleeding for 9-16d. Eight percent of treated women bleed 30d or more. The duration of bleeding increases with gestational age at termination. There are only a few randomized studies comparing medical and surgical termination, and the definitions of successful outcome (complete abortion), adverse effects, and complications vary. The three most common reasons a woman chooses a medical abortion are ??avoidance of surgery,?? ??avoidance of general anesthesia,?? and ??the method being more natural.?? The duration of bleeding, degree of blood loss, and frequency of uterine pain, vomiting, and diarrhea are all greater with mifepristone abortion. Conversely, the incidence of major complications such as blood transfusion and pelvic infection does not seemingly differ between the two. Surgical complications, such as uterine perforation and cervical tears, are less common in women who choose medical abortion. Mifepristone helps preserve fertility and avoid major maternal complications (death, hysterectomy) in women with either cervical or uterine scar ectopic pregnancy. At term, mifepristone has a modest impact on cervical ripening if given 24h before labor induction. Mifepristone appears to reduce the need for misoprostol and oxytocin compared with placebo.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Mifepristone does cross the primate placenta. The human experience with continued

Pregnancy

after failed medical termination is limited. Normal outcomes are reported. While Mo?bius? syndrome is increased after failed misoprostol termination, the same cannot be said for mifepristone.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether mifepristone enters human breast milk. Rodent studies suggest that mifepristone enhances lactation.

Pregnancy

. There are no reports of miglitol in pregnant women. Because it inhibits glucose absorption, miglitol is additive to the hypoglycemic effect of other agents such as sulfonylureas. There is no evidence that systemic absorption contributes to its effect. Insulin is the currently recommended hypoglycemic agent of choice during pregnancy, though a growing body of work suggests a promising future for some oral hypoglycemic agents.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether miglitol crosses the human placenta. Considering poor absorption, it is unlikely the 723 maternal systemic concentration will reach a clinically relevant level. Rodent studies are reassuring, revealing no evidence of teratogenicity, though there was a small increase in IUGR at doses in multiples of those used clinically. Placental transport studies in the rat indicate limited transport even after parenteral administration.

Breastfeeding

There is no published experience in nursing women. The Breastfeeding newborn is exposed to less than 0.5% of the maternal dose of miglitol, a dose that should not have a clinically relevant effect on the neonate.

Pregnancy

. Milrinone is an inotropic agent for the short-term management of CHF. The published experience during

Pregnancy

is limited to case reports, typically in women with pulmonary hypertension and myocardial decompensation. The results have been mixed.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether milrinone crosses the human placenta. While milrinone does cross the baboon placenta, placental transfer in the ewe is low. In the latter, milrinone increases uterine blood flow. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. There was some evidence of embryotoxicity at high doses in rabbits.

Breastfeeding

There is no published experience in nursing women. It is unknown whether milrinone enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of minocycline in pregnant women. Case reports note its use for the treatment of recurrent pemphigoid gestations. Similar to other tetracyclines, concern has been raised that it might lower the effectiveness of low-dose oral contraceptive agents. (See Tetracycline.)

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether minocycline crosses the human placenta. It is unlikely the maternal systemic concentration will reach a clinically relevant level if applied topically for acne. Other tetracyclines cross the human placenta and are associated with tooth discoloration and, in rodents, increased embryo resorption. (See Tetracycline.)

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether minocycline enters human breast milk. Milk discoloration is reported. (See Tetracycline.)

Pregnancy

. There are no adequate reports or well-controlled studies of minoxidil in pregnant women. Minoxidil is no longer often used for the treatment of hypertension, but rather is used for balding. Balding can be a normal physiologic occurrence in women taking oral contraceptives or after parturition. It can be treated with either progesterone or minoxidil. Less than 2% of the topical dose is absorbed systemically.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether minoxidil crosses the human placenta. Caudal regression syndrome was reported in a mother taking minoxidil long before and during gestation. Fetal hypertrichosis is also reported in fetuses whose mothers used minoxidil topically throughout pregnancy. Rodent studies are 727 reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxicity was seen with high doses.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Minoxidil enters human breast milk, achieving a peak concentration of 50mcg/L 2h after 7.5mg PO. It is unlikely that topically administered drug would result in a clinically relevant milk concentration.

Pregnancy

. Depression is common during and after pregnancy, but typically goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. Mirtazapine is one option for patients unresponsive to or intolerant of SSRIs. Most of the published experience with mirtazapine during

Pregnancy

is limited to small case series and epidemiologic surveys.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether mirtazapine crosses the human placenta. Based on reports from Teratogen Information Services, mirtazapine does not appear to increase the baseline rate of major malformations of 1-3%. However, there is an increase in spontaneous losses similar to that reported for other antidepressants. Further, there is a single case report of recurrent neonatal hypothermia through 10d of life.

Breastfeeding

Mirtazapine enters human breast milk. Mean relative infant doses for mirtazapine and desmethylmirtazapine were 1.5% and 0.4%, respectively. The mean M:P ratio was 1.1 for mirtazapine and 0.6 for desmethylmirtazapine. Mirtazapine was detected (1.5mcg/L) in only 1 of 4 infants tested.

Pregnancy

. Misoprostol is a prostaglandin E analog. The only FDA-approved indication is the treatment and prevention of intestinal ulcer disease resulting from NSAID drug use. Although still not approved by the FDA for other indications, misoprostol is well studied and widely used for both cervical ripening and the induction of labor during either the 2nd or 3rd trimesters. The route of administration is relevant. At 2min after 600mcg PO in postpartum women, the plasma level is 91.5pg/ml; it peaks at 20min (344pg/ml), and then falls steeply by 120min (27.8pg/ml). Misoprostol administered PR generates lower peak levels and a reduction in the prevalence of adverse effects compared with oral drug. The AUC for rectal misoprostol is higher by 121pg/h/ml than oral drug; the mean maximum serum concentration is also significantly lower and occurs >20min later than it does for oral drug. Women reported shivering after administration: 76% after 600mcg PO, 56% after 400mcg PR, and 54% after 600mcg PR. The relative risk of shivering in both PR groups is 25% lower than in the PO group. Severe shivering is reduced by 70% in PR groups. Increasing rectal doses may achieve higher efficacy without reducing the acceptability of the treatment. Early to mid-

Pregnancy

termination: Combined with mifepristone, misoprostol is safe and effective for medical termination of early pregnancy. Typically, misoprostol is given PV 48h after mifepristone. The administration of either 2 doses of misoprostol (400mcg) or one dose (800mcg) after mifepristone significantly reduces the risk of failed abortion compared to mifepristone alone. Vaginal misoprostol shortens the time from induction to delivery compared to PO. A wide range of dosing regimens has been suggested for 2nd trimester termination; 400mcg PO or 400mcg PV q4-6h are common. Dosing regimens for the induction of labor generally decrease with advancing gestation (e.g., vaginal misoprostol: 13-17w, 200mcg q6h; 18-26w, 100mcg q6h; and greater than 27w, 25-50mcg q4h). Misoprostol does not reduce the blood loss and the time for placental expulsion after 2nd trimester termination. Term pregnancy: Misoprostol is commonly used to induce cervical ripening and labor. In August 2000, the manufacturer issued a warning letter to American health care providers cautioning against the use of misoprostol in pregnant women secondary to the lack of safety data for its use in obstetric practice. The ACOG took issue with that position, as there were a multitude of studies supporting its use. Misoprostol is effective in ripening the cervix and inducing labor at term when given either PV or PO. It is inexpensive and stable at room temperature. Debate continues on the optimal dose, regimen, route of administration, and concurrent use of ancillary ripening methods (laminaria, Foley balloon, dinoprostone gel). Low-dose misoprostol (25mcg) is effective for cervical ripening and labor 730 induction. More recently, a single 25mcg outpatient intravaginal dose of misoprostol was reported to be effective in decreasing the interval to delivery in women with unfavorable cervices at term. The study, however, was inadequately powered to provide strong comment on safety. Uterine tachysystole is more common after 50mcg or more given vaginally or orally. Clinical trials report increased frequencies of meconium passage

Breastfeeding

Orally administered misoprostol is secreted in colostrum within 1h, but it is essentially undetectable by 5h. The AUC is only 51.4pg/h/ml, or1=6 of the maternal AUC. It has not been studied in women with established lactation. Though misoprostil is 731 rapidly metabolized, there is no information on whether its active metabolite is excreted.

Pregnancy

. Mitomycin is an alkylating agent used as adjunct therapy and is not recommended as single-agent, primary therapy. There are no adequate reports or well-controlled studies of mitomycin in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether mitomycin crosses the human placenta. It crosses the rodent placenta in a limited fashion, reaching F:M ratios less than 10%. In rodents, mitomycin is a potent teratogen damaging the preimplantation blastocyst, leading to embryo loss. Later exposure produces a myriad of bony malformations. Its effect is enhanced by caffeine. There are no reports in humans. 733

Breastfeeding

There is no published experience in nursing women. It is unknown whether mitomycin enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of mitoxantrone in pregnant women. The published experience is limited to several case reports. More recently, mitoxantrone has been advocated as a treatment for MS, a disease common in reproductive-age women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether mitoxantrone crosses the human placenta. In the single report of 1st trimester use, the neonate was growth restricted. Rodent studies are reassuring, 734 revealing no evidence of teratogenicity, but the doses studied were too low.

Breastfeeding

There is no published experience in nursing women. Mitoxantrone enters human breast milk, reaching a significant concentration, though the kinetics remain unclear. It should probably be considered incompatible with Breastfeeding pending additional study.

Pregnancy

. The published experience with modafinil during

Pregnancy

is limited to a case report. Modafinil is an inducer of CYP enzymes. Thus, the effectiveness of oral contraceptives may be reduced during therapy and for 1mo after discontinuation. MS is fairly common in reproductive-age women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether modafinil crosses the human placenta. Adequate rodent teratogenicity studies have not been performed. Those that have been done suggest an increased rate of embryotoxicity. The manufacturer reports 7 exposures during

Pregnancy

without apparent adverse effects. 735

Breastfeeding

There is no published experience in nursing women. It is unknown whether modafinil enters human breast milk.

Pregnancy

. There is no published experience with moexipril during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether moexipril crosses the human placenta. Other inhibitors of the renin-angiotensin system cross and can cause fetal renal failure. They are generally considered contraindicated during

Pregnancy

unless there is no other therapeutic option. The same is true for moexipril.

Breastfeeding

There is no published experience in nursing women. It is unknown whether moexipril enters human breast milk.

Pregnancy

. Acute schizophrenia presents several difficult management decisions during pregnancy, and a careful risk:benefit analysis is required. There are no adequate reports or well-controlled studies of molindone in pregnant women. The published experience consists of isolated case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether molindone crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether molindone enters human breast milk.

Pregnancy

. Allergic rhinitis affects1=3 of women of childbearing age. There are no adequate reports or well-controlled studies of mometasone in pregnant women. This agent offers the potential advantage of once-daily dosing. However, budesonide is generally considered the preferred agent.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether mometasone crosses the human placenta. There are no documented epidemiologic studies with IN corticosteroids (e.g., budesonide, fluticasone, mometasone) during pregnancy. However, inhaled corticosteroids (e.g., beclomethasone) are not incriminated as teratogens. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level.

Breastfeeding

There is no published experience in nursing women. It is unknown whether mometasone enters human breast milk. However, considering the indications, dose, and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. Moricizine is a phenothiazine derivative with class IC antiarrhythmic properties. It undergoes extensive first-pass metabolism, has a bioavailability of 34-38%, and is extensively plasma bound. There is no published experience with moricizine during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether moricizine crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Moricizine enters human and rodent breast milk, but the kinetics remain to be elucidated.

Pregnancy

. Morphine is one of the most frequently used opioids for pain control during human parturition. The elimination t/2 of morphine is shorter and the plasma clearance quicker in parturients than in nonpregnant women. Morphine as part of an epidural or PCA regimen is common. It is also administered intrathecally after cesarean section for relief of postoperative pain for the first 48h. XR epidural morphine provides superior and prolonged postcesarean analgesia compared to conventional epidural morphine with no significant increases in adverse events. The addition of small dose to the spinal component of the continuous spinal epidural improves the effectiveness of epidural labor analgesia and reduces the need for pain medications over 24h, but results in a small increase in nausea. Epidural morphine significantly reduces the incidence of headache and the need for a blood patch after dural puncture. There is a long clinical experience supporting the relative safety of morphine for the listed indications. The combination of small doses of opioids and bupivacaine for spinal anesthesia eliminates intraoperative discomfort and reduces postoperative analgesic requirements in women undergoing either vaginal or cesarean delivery. The two most frequently used agents are fentanyl and morphine. The intrathecal injection of 150mcg intensifies the intraoperative hypothermic effect of bupivacaine spinal anesthesia for cesarean section patients. PCA, which provides pain relief through 741 self-administration of IV doses of opioids, is widely available and advocated as an effective analgesic modality. Morphine PCA offers a good quality of analgesia with minimal Side effects include addiction, seizures, respiratory depression, hypotension, shock, apnea, cardiac arrest, bradycardia, toxic megacolon, ileus, abdominal pain, miosis, itching, dry mouth, decreased libido, biliary spasm, paresthesias, pruritus, itching, flushing, urinary retention, and asthenia.

Fetal Health

Morphine readily crosses the term human placenta. Rapid maternal clearance shortens the fetal exposure. The concentration of free morphine in umbilical venous blood after delivery is significantly associated with the dose-delivery interval and has a significant effect on the need for neonatal resuscitation. Alterations in fetal biophysical profile parameters such as fetal breathing movements and fetal heart rhythm should be expected as morphine decreases fetal heart variability and breathing frequency. It is not clear whether morphine decreases gross or fine fetal movements. Placental retention of morphine may prolong fetal exposure, explaining at least in part its prolonged effect on fetal behavior relative to the maternal concentration. Morphine has been combined with benzodiazepines (e.g., diazepam) for the relief of pain and anxiety during fetal surgical procedures. While there is no evidence morphine is a human teratogen, uncontrolled retrospective studies of neonates chronically exposed to other opioids note reduced brain volume at birth that normalizes during the 1st month of life. Infants born to opioid-abusing mothers are more often SGA, and have decreased ventilatory responses to CO2and increased risk of SIDS. Neonatal abstinence syndrome due to opiate withdrawal produces sleep/wake abnormalities, feeding difficulties, weight loss, and seizures. Rodent teratogen studies have not been performed. Other rodent studies suggest in utero exposure causes long-term alterations in adult brain and behavior. These changes affect both the NE and opioid systems of several brain areas, including those involved in memory, stress responses, and the maintenance of homeostatic balance with the external environment. Breastfeeding Morphine is excreted in human breast milk, and the M:P AUC ratio after parenteral administration approximates 2.5:1. The amount taken by the neonate depends on the maternal plasma concentration, quantity of milk ingested, and the extent of first- pass metabolism. In general, morphine is preferred to meperidine in

Pregnancy

. There is no published experience with moxifloxacin during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether moxifloxacin crosses the human placenta. Animal studies in rodents and dogs reveal that fetal exposure to quinolone antibiotics is associated with an acute arthropathy of the weight-bearing joints. Although arthropathy has only rarely been observed in humans, the toxicity observed in immature animals has led to the restricted use of quinolones in pregnant women. There was no evidence of teratogenicity in monkeys fed 2.5the MRHD, though there was an increase in IUGR. Recent studies conclude that the use of fluoroquinolones during embryogenesis is not associated with an increased risk of major malformations.

Breastfeeding

There is no published experience in nursing women. It is unknown whether moxifloxacin enters human breast milk. It is excreted into rodent milk.

Pregnancy

. There is no published experience with nabumetone during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether nabumetone crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. There is evidence, however, of increased embryo resorption.

Breastfeeding

There is no published experience in nursing women. It is unknown whether nabumetone enters human breast milk.

Pregnancy

. Nadolol is a nonselective b-blocker offering the advantage of once-daily dosing. There are no adequate reports or well- controlled studies of nadolol in pregnant women. The published literature is limited to scattered case reports. In one instance, it was used to treat hypertension associated with primary hyperaldosteronism.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether nadolol crosses the human placenta. Other drugs in this class do cross. Scattered case reports suggest fetal exposure may increase the risk of cardiorespiratory depression, mild hypoglycemia, and IUGR. The long duration of action of nadolol and the fact that it is only 30% protein bound make it less desirable during

Pregnancy

than other b-blockers such as propranolol. Nadolol crosses the rodent placenta. Rodent studies are generally reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. There is evidence of embryotoxicity and IUGR.

Breastfeeding

Nadolol is excreted into human breast milk. It is estimated the nursing newborn would ingest 2-7% of the daily maternal dose. Thus, there is a small but real potential for a clinical effect depending upon neonatal clearance. If a woman elects to continue nursing while taking nadolol, the child should be observed for evidence of b blockade.

Pregnancy

. Nafcillin is a penicillinase-resistant penicillin eliminated primarily by nonrenal routes, namely hepatic inactivation and excretion in the bile. There are no adequate reports or well-controlled studies of nafcillin in pregnant women. The published literature consists of scattered case reports. Other penicillins have proved safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether nafcillin crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether nafcillin enters human breast milk. It is generally considered compatible with breastfeeding. Nafcillin is frequently used for the treatment of mastitis of cows.

Pregnancy

. There is no published experience with naftifine during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether naftifine crosses the human placenta. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether naftifine enters human breast milk. However, considering the dose and route, it is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Nalbuphine (formerly marketed as Nubain) is a synthetic opioid agonist-antagonist analgesic commonly used for intrapartum analgesia. Its potency is essentially equivalent to morphine on a milligram basis. Nalbuphine acts within minutes after IV administration, and <15min after SC or IM injection; the duration of analgesia ranges from 3 to 6h. There are no well- controlled studies of nalbuphine in pregnant women. It is, however, a popular agent for analgesia during labor, comparable to meperidine. Concerns for fetal safety were raised by a pharmaceutical company that no longer manufactures nalbuphine (see http://www.fda.gov/medwatch/safety/2005/aug_PI/ Nubain_PI.pdf). There is insufficient information to support these concerns or to recommend any change in the administration of this medication for analgesia in labor. Due to its ability to bind the same opiate receptor as morphine, IV nalbuphine is sometimes used for the treatment of intrathecal morphine- induced pruritus after cesarean delivery.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Nalbuphine crosses the human placenta, achieving an F:M ratio approximating 0.75. Nalbuphine decreases the number of FHR accelerations and variability, but does not affect the fetal response to vibroacoustic stimulation. The neonatal t/2 is estimated at 4h. Nalbuphine can cause respiratory depression, and should be used with caution in women delivering preterm. Rodent studies are reassuring, revealing no evidence of 751 teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

The mean and maximum nalbuphine milk concentrations are 42 ? 26 and 61 ? 26ng/ml, respectively. Assuming a milk volume of 150ml/kg/d, the mean and maximum doses a breastfed neonate would ingest in 1 day are 7.0 ? 3.2 and 9.0 ? 3.8mcg/kg/d. That equates to a relative infant dose of 0.59 ? 0.27% of the weight- adjusted maternal daily dose.

Pregnancy

. Asymptomatic bacteriuria is common during pregnancy. Perhaps 1=3 of affected pregnant women will develop symptomatic disease (hemorrhagic cystitis or pyelonephritis). Nalidixic acid is one treatment alternative for asymptomatic bacteriuria of pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Nalidixic acid crosses the human placenta, though the kinetics remain to be elucidated. Rodent and canine teratogenicity studies reveal the older quinolones such as nalidixic acid, flumequine, and pipemidic acid are associated with acute arthropathy of the weight-bearing joints. Although arthropathy is rare in adult humans, toxicity was observed in immature animals, leading to the restricted use of these agents during pregnancy. More recent studies conclude that nalidixic acid is not associated with any increased risks of spontaneous abortion, prematurity, IUGR, or postnatal disorders. A small increase in the risk of pyloric stenosis cannot be excluded.

Breastfeeding

Nalidixic acid is excreted into human breast milk. However, the nursing newborn would ingest <0.05% of the maternal dose.

Pregnancy

. Nalmefene is a long-acting opioid antagonist used for the treatment of overdose. It was also used to provide long-term relief from Side effects include arrhythmia, tachycardia, bradycardia, fever, postoperative pain, N/V, headache, vasodilation, dizziness, somnolence, confusion, and chills.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether nalmefene crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Breastfeeding There is no published experience in nursing women. Nalmefene is excreted into human breast milk, though the kinetics remain to be elucidated. However, considering the indication and dosing, one-time nalmefene use is unlikely to pose a clinically significant risk to the

Pregnancy

. Naloxone is a popular opioid antagonist. Pregnant heroin users have poor maternal and neonatal outcome. Medically supervised heroin withdrawal is generally discouraged during

Pregnancy

because of the fetal risk and a high likelihood of failure with return to regular illicit heroin use. More recently, a number of withdrawal procedures developed using naloxone or naltrexone have met with some success in users who continue the antagonist throughout pregnancy. Maternal respiratory arrest is a rare but potentially life-threatening complication associated with intrathecal opioids for labor analgesia. Resuscitation should include IV naloxone. Very-low-dose IV naloxone is often used to treat neuraxially-injected morphine-associated pruritus. It is not effective when given SC as prophylaxis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether naloxone crosses the human placenta. Naloxone does not alter the placental transfer or clearance of morphine in humans. Neonates of women given parenteral opioids in labor that require naloxone have lower 1min Apgar scores than neonates whose mothers have epidural analgesia. Physicians practicing in community vs. university hospitals use naloxone more often to resuscitate the neonate. It is unclear whether this increased use reflects adherence to the American Academy of Pediatrics? guidelines for resuscitation, or whether the neonates delivered in community hospitals require resuscitation more frequently. Either way, it is clear this practice is poorly supported and should be examined. Porcine studies suggest that increased opioid ??tonus?? lowers the FHR and decreases fetal movement. Naloxone antagonizes the inhibitory effect of morphine on fetal heart rhythm and stimulates fetal hypermotility. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether naloxone enters human 755 breast milk. However, considering the indication and dosing, one-time naloxone use is unlikely to pose a clinically significant risk to the Breastfeeding neonate. Endogenous opioids inhibit oxytocin neurons until parturition, and naloxone increases oxytocin secretion in pregnant rats. In humans, oxytocin secretion is inhibited in

Pregnancy

. Naltrexone is a synthetic congener of oxymorphone with no opioid agonist properties. There are no adequate reports or well-controlled studies of naltrexone in pregnant women. Pregnant heroin users have poor maternal and neonatal outcome. Medically supervised heroin withdrawal is generally discouraged during

Pregnancy

because of the fetal risk and a high likelihood of failure with return to regular illicit heroin use. Recently, a number of withdrawal procedures developed using naloxone or naltrexone have met with some success in users who continue the antagonist throughout pregnancy. More recently, implants have been studied as a vehicle for sustained release. Ovarian failure of hypothalamic origin is a consequence of an inappropriate increase in opioid tone of the neurons that release GnRH in a pulsatile manner. Naltrexone administration to these women can lead to pregnancy. After cesarean section, naltrexone is effective against the pruritus and vomiting associated with intrathecal morphine for analgesia, but shortens the duration of analgesia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Naltrexone crosses the human and rodent placenta. Rodent studies are generally reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. There is evidence of embryo and early fetal toxicity. Rodents exposed to naltrexone during prenatal life are larger in weight and length, confirming that native opioids are important growth-inhibiting regulators. Naltrexone has no behavioral affect on exposed rabbit pups.

Breastfeeding

The excretion of naltrexone and its primary metabolite 6,b-naltrexol has been measured in breast milk in one patient?an opiate addict undergoing oral naltrexone pharmacotherapy (5mg/d). The calculated infant dose relative to the maternal weight was 0.03% for naltrexone and 0.83% (as naltrexone equivalents) for 6,b-naltrexol. Total relative infant dose estimated for the complete 24h dose interval was 1.06%. Only 6,b-naltrexol was detected in infant plasma and at a very low concentration of 1.1mcg/L. These levels should pose little risk to the newborn.

Pregnancy

. There are no adequate reports or well-controlled studies of naphazoline in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether naphazoline crosses the human placenta. Considering the dose and route, it is unlikely the associated maternal systemic concentration will reach a clinically relevant level.

Breastfeeding

There is no published experience in nursing women. It is unknown whether naphazoline enters human breast milk. However, considering the indication and dosing, occasional naphazoline use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. NSAIDs are widely distributed in OTC preparations, and their use during

Pregnancy

is underestimated. About 5% of women report use of either ibuprofen or naproxen near conception or during pregnancy. It may be combined with sumatriptan for the treatment of acute migraine. In a recent prospective case-control study, prenatal ibuprofen or naproxen use increased the risk of spontaneous abortion by 80% (adjusted hazard ratio 1.8 [95% CI 1.0-3.2]). The association was stronger if the initial use was around conception or if the use lasted more than 1w. Naproxen offers no distinct clinical advantage after the 1st trimester over other NSAIDs on the market. It provides analgesic relief similar to acetaminophen after vaginal delivery. One randomized trial suggests the addition of regular doses of naproxen to prn requests for acetaminophen-codeine provides small reductions in 759 pain on day 2 after cesarean delivery, with the greatest effects at 36h, when pain typically peaks.

Fetal Health

Naproxen crosses the human placenta, achieving an F:M ratio of 0.92 during the 2nd trimester. Fetal levels are dependent on the maternal, as NSAIDs are not metabolized by the fetal kidney. Other NSAIDs can cause premature closure of the fetal ductus arteriosus. While the ductal response to naproxen remains to be studied, there are several case reports of neonatal pulmonary hypertension after its use in the 3rd trimester. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Although naproxen is excreted into human breast milk, the amount of drug transferred is only a small fraction of the maternal dose and should not pose a risk to the nursing newborn.

Pregnancy

. There are no adequate reports or well-controlled studies of dantrolene in pregnant women, though it has been used for both the prevention and treatment of acute malignant hyperthermia and neuroleptic malignant syndrome, where it may be lifesaving. However, prevention of malignant hypertension is not usually recommended. Instead, a nontriggering anesthetic should be selected.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It readily crosses the placenta, achieving equal maternal and fetal whole blood levels by delivery. No adverse neonatal effects are reported. Dantrolene is embryocidal in rodents when administered at a multiple of the MRHD.

Breastfeeding

Dantrolene is excreted in human breast milk, but the peak concentration reported is small and unlikely to produce neonatal levels as high as fetal levels. Though the kinetics remain to be detailed, dantrolene is likely compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of dapsone in pregnant women. Dapsone, alone or in combination with pyrimethamine, trimethoprim-sulfamethoxazole, or pentamidine, is the most commonly used drug for PCP prophylaxis. Dapsone should be administered in combination with one or more antileprosy drugs to avoid resistance. Dapsone should also be considered during

Pregnancy

in areas where P. falciparum resistance to chloroquine and pyrimethamine- sulfadoxine is rapidly increasing. Mild degrees of hemolysis occur consistently with continued therapy but may be less likely with intermittent treatment. Most reported adverse effects have occurred after long-term use.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Transfer across the human placenta likely occurs, as there are reports of neonatal methemoglobinemia after maternal dapsone. Dapsone appears unassociated with fetal abnormalities in humans. Rodent teratogenicity studies have not been performed.

Breastfeeding

Dapsone is excreted in breast milk in substantial amounts, with the unsupplemented breastfed infant receiving some 15% of the maternal dose. Hemolytic reactions can occur in newborns. Caution is advised. Breastfeeding is contraindicated in HIV- infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. Daunorubicin is an anthracycline antibiotic. Daunoxome is an encapsulated form designed to maximize selectivity for solid tumors such as Kaposi?s sarcoma. The specific mechanism by which the daunorubicin citrate liposome delivers the drug to solid tumors is not known. It is also commonly used in combination with other drugs for the treatment of breast cancer. There are no adequate reports or well-controlled studies of daunorubicin in pregnant women. There are multiple reports of its use during

Pregnancy

with a successful outcome.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Daunorubicin crosses the human placenta, but in the isolated perfused model the global transfer was <3%. Not surprisingly, there are multiple reports of its use during pregnancy, including 1st trimester, either without evidence of an adverse fetal effect or, on occasion, with a report of anemia, thrombocytopenia, and neutropenia. Though children (and presumably fetuses) have greater sensitivity to the cardiotoxic effects of daunorubicin than adults, there are no such reports in exposed fetuses. Short-term follow up has been encoraging. Rodent studies reveal, at doses a fraction of those used in the human, an increased prevalence of anophthalmia, microphthalmia, and incomplete ossification when given alone, and esophageal atresia with tracheoesophageal fistula if daunorubicin is combined with doxorubicin.

Breastfeeding

Daunorubicin is excreted into human breast milk, but in the only case reported, the total amount delivered in the milk (maximum concentration of active antibiotic: 0.24mg/L) was negligible.

Pregnancy

. There are no adequate reports or well-controlled studies of deferoxamine in pregnant women. There are case reports of its use during

Pregnancy

and lactation in women with transfusion- dependent homozygous b-thalassemia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether deferoxamine crosses the human placenta. However, there are over 50 published cases without evidence of adverse fetal effects. One recent case suggested decreased fetal iron. Rodent studies reveal an increased incidence of delayed ossification and skeletal anomalies when administered at multiples of the MRHD.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether deferoxamine enters human breast milk. Case reports suggest deferoxamine therapy does not alter the iron content of human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Because delavirdine increases the plasma concentrations of several protease inhibitors, it may also be beneficial as a component of salvage therapy in combination with protease inhibitors.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether delavirdine crosses the human placenta. In rodents, delavirdine causes embryotoxicity and VSDs at doses that are multiples of the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether delavirdine enters human breast milk. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. Demecarium is a cholinesterase inhibitor with sustained activity. It produces miosis and ciliary muscle contraction, and should be used only when shorter acting miotics have proved inadequate. There is no published experience with demecarium during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether demecarium crosses the placenta. Considering the dose and route, it is unlikely the maternal systemic concentration will reach clinically relevant level. Rodent teratogenicity studies have apparently not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether demecarium enters human breast milk. However, considering the indication and dosing, demecarium use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. There are no adequate reports or well-controlled studies of demeclocycline during pregnancy. Outside of pregnancy, demeclocycline may cause diabetes insipidus?like syndrome (polyuria, polydipsia, and weakness) that is nephrogenic in origin, dose-dependent, and reversible on discontinuation.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether demeclocycline crosses the human placenta. Other tetracyclines may cause a permanent discoloration of the teeth (yellow-gray/brown teeth) when given during the latter half of pregnancy, or during childhood prior to 8 years of age. In rodents, exposure to demeclocycline is associated with tooth discoloration. Exposure to other tetracyclines is associated with delayed bone growth.

Breastfeeding

There is no published experience in nursing women. It is unknown whether demeclocycline enters human breast milk. It likely enters human breast milk, as do other tetracyclines, and is generally considered incompatible with breastfeeding.

Pregnancy

. Depression is a commonly overlooked and undertreated disorder during

Pregnancy

and the puerperium.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. Women with a history of depression are at high risk for recurrence during

Pregnancy

and the puerperium. TCAs continue to be widely used during pregnancy, but remain inadequately studied. Desipramine is a metabolite of imipramine. Desipramine lowers the threshold for seizures. There are no adequate reports or well-controlled studies of desipramine in pregnant women. There are marked interindividual differences during

Pregnancy

in the metabolism of TCAs. TCAs are effective for the treatment of postpartum depression.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether desipramine crosses the human placenta. No evidence of teratogenicity is seen in rhesus monkey fetuses exposed to imipramine despite a high incidence of maternal toxicity and abortion. A large body of study on the impact of in utero exposure to desipramine on postnatal neurologic function is inconclusive.

Breastfeeding

Desipramine is excreted in small quantities into human breast milk, but is not detectable in the blood of Breastfeeding newborns. No adverse effects are reported in

Pregnancy

. The metabolic clearance rate of AVP increases 4-fold during human pregnancy. As opposed to natural hormone, 269 desmopressin (1-deamino-[8-D-arginine]vasopressin) has no uterotonic action in antidiuretic doses. It is the treatment of choice for most patients with type I vWD. Types II and III are usually unresponsive, and best treated with either FFP or concentrates containing von Willebrand factor. There is a high risk of delayed postpartum hemorrhage in vWD type I, especially during the first week. The risk is independent of the factor VIII level during the 3rd trimester, and reflects the rapid clearance of the various factor VIII components postpartum. The risk of postpartum hemorrhage is especially high in women with type II or III vWD, and desmopressin is effective prophylaxis in responsive women. Hemorrhage may occur up to 5w postpartum. Administer desmopressin at least 30min prior to a surgical procedure to maintain hemostasis during the procedure and immediately postoperatively. It is also effective treatment for women who develop transient diabetes insipidus during late

Pregnancy

and/or the immediate puerperium. Maternal desmopressin use reduces and stabilizes plasma osmolality and increases AF volume. It has been proposed as a possible treatment of oligohydramnios and, if given intra-amniotically, polyhydramnios.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. There is no detectable transfer of desmopressin at therapeutic maternal drug concentrations. No adverse fetal effects are reported when desmopressin is used during human pregnancy. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. In sheep, intra-amniotic desmopressin inhibits fetal urination without CV effect or change in fetal swallowing.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. A single study found minimal desmopressin in human breast milk after a single nasal spray. Considering the dose and dosing frequency, it seems unlikely a significant quantity would reach the Breastfeeding neonate. It has been used to treat diabetes insipidus during the puerperium.

Pregnancy

. Dexamethasone is used widely during

Pregnancy

for the acceleration of fetal lung maturity. A comparison of PO (8mg) versus IM (6mg) dosing reveals similar bioavailability as determined by the AUC and terminal t/2s. Most large studies conclude the risk of maternal infection in women after PPROM is not increased by dexamethasone. It may transiently cause an abnormal glucose tolerance test, and will worsen diabetes mellitus. Large doses such as those given to hasten the fetal lung maturation are associated with pulmonary edema, especially when combined with a tocolytic agent in the setting of an underlying infection. Dexamethasone does not reduce the maternal perception of fetal movements and short-term variability. It is not contraindicated in women with severe preeclampsia requiring preterm delivery. Women chronically treated must be monitored closely for hypertension or glucose intolerance, and treated with stress replacement doses postoperatively and postpartum. Dexamethasone is an effective antiemetic after general anesthesia for

Pregnancy

termination. There are as yet uncorroborated reports that IV dexamethasone helps modify the clinical course of the so-called HELLP syndrome both ante- and postpartum. It may also reduce itching in women with intrahepatic cholestasis of pregnancy.

Fetal Health

Antenatal corticosteroid administration is the only therapy conclusively demonstrated to reduce the perinatal morbidity and death associated with preterm delivery. Newborns of treated women have lower incidences of RDS, NEC, and IVH and shorter hospital stays. Therapy for pulmonary maturity should be limited to no more than 2 courses. The route of administration is apparently important, as neonatal outcome is worse when dexamethasone is given PO compared to IM to hasten lung maturation. Dexamethasone readily crosses the human placenta unmetabolized. Infants of women treated chronically should be carefully observed for signs of hypoadrenalism. Complete fetal heart block has been treated with dexamethasone with positive result. Some studies suggest that, in contrast to betamethasone, dexamethasone does not alter biophysical parameters of the fetus (i.e., fetal breathing) when administered for the enhancement of lung maturation. However, oligohydramnios is reportedly more common. When initiated by 6-7w, dexamethasone can prevent or diminish virilization due to congenital adrenal hyperplasia. PO dosing is equal to IM for the suppression of unconjugated estriol levels in the 3rd trimester. It is continued until a definitive diagnosis is established by DNA analysis of chorionic villi at 11- 13w. One observational study concluded that children subjected to multiple antenatal doses of dexamethasone to enhance pulmonary maturity were more likely to develop leukomalacia and neurodevelopmental abnormalities at 2y old than those treated with either betamethasone or single doses of dexamethasone. This remains to be confirmed. Some suggest emotional stress during organogenesis can cause congenital malformations by increasing the level of cortisone. Corticosteroids produce oral clefting in some rodents. Some epidemiologic studies conclude, after controlling for confounding 272 factors, that prenatal exposure to corticosteroids adds a 6-fold increase in the risk for cleft lip with or without cleft palate, IUGR, and shortening of the head and mandible. In contrast, the Collaborative Perinatal Project followed women treated during the 1st trimester. While the number of exposures was limited, no increase in congenital malformations was detected. There was no increased risk of anomalies after organogenesis. Antenatal dexamethasone f

Breastfeeding

There are no adequate reports or well-controlled studies in Breastfeeding women. Dexamethasone is excreted into human breast milk, but it is unclear whether maternal treatment increases the concentration of cortisone in breast milk.

Pregnancy

. Dexchlorpheniramine is the active metabolite of chlorpheniramine. There are no adequate reports or well- controlled studies in pregnant women, and its safety during

Pregnancy

is not established. However, chlorpheniramine is widely available in OTC preparations and has not been implicated with adverse effects during pregnancy.

Fetal Health

Dexchlorpheniramine has not been incriminated as a human teratogen. (See Chlorpheniramine.)

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether dexchlorpheniramine enters human breast milk. There are no reports of adverse effects on the Breastfeeding neonate despite widespread availability.

Pregnancy

. There are no adequate reports or well-controlled studies of dexmedetomidine in pregnant women. Dexmedetomidine enhances rat myometrial contractility in vitro.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Dexmedetomidine crosses the human placenta, which also binds a large fraction, delaying transfer. Rodent studies are generally reassuring, revealing no evidence of teratogenicity, though embryotoxicity and IUGR occurs in some models. It is a potent neuroprotector that has been explored in perinatal models.

Breastfeeding

There is no published experience in nursing women. It is unknown whether dexmedetomidine enters human breast milk. Dexmedetomidine is excreted into rodent milk. Considering its indications, it is unlikely to pose a clinically significant risk to women who choose to breastfeed.

Pregnancy

. There are no published reports of dexmethylphenidate use during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dexmethylphenidate crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity, though delayed ossification is seen at the highest dose level. However, there is concern that antenatal exposure may lead to behavioral abnormalities based on rodent and human study of related drugs (amphetamine and methamphetamine).

Breastfeeding

There is no published experience in nursing women. It is unknown whether dexmethylphenidate enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of dextroamphetamine in pregnant women. There are case reports of its use for the treatment of narcolepsy during pregnancy. Since amphetamines are used to decrease appetite and maintain adequate body weight, its usage during

Pregnancy

should be discouraged once

Pregnancy

is diagnosed.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Amphetamines cross the human placenta. One case report describes severe congenital body deformity, tracheoesophageal fistula, and anal atresia in the newborn of a mother who took dextroamphetamine throughout the 1st trimester. Epidemiologic study reveals that birth weight is unaffected if discontinued prior to 28w, but is significantly lower if discontinued later. Mouse transport is also confirmed (approximately 18% after 1h). Dextroamphetamine is embryotoxic and teratogenic when administered to some but not all rodents.

Breastfeeding

Amphetamines are excreted in human milk and are generally considered incompatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of dextromethorphan in pregnant women. It is commonly found in many OTC preparations. No adverse

Pregnancy

outcomes are associated with its use.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dextromethorphan crosses the human placenta. The wide and long-term clinical experience suggests any fetal risk of dextromethorphan-containing cough preparations is small. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than that used clinically. Several rodent studies suggest dextromethorphan may have a beneficial effect on the developing brain chronically exposed to morphine. Dextromethorphan is a teratogen in the chick embryo, a poor model for such studies.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether dextromethorphan enters human breast milk. However, the wide and long-term clinical experience suggests any risk to the Breastfeeding neonate is small.

Pregnancy

. Dextrothyroxine is the dextrorotatory isomer of thyroxine. There is a single report of its use during

Pregnancy

in the successful treatment of thyroid hormone resistance syndrome (RTH). RTH is characterized by an elevated serum thyroxine, inappropriately ??normal?? TSH, and reduced thyroid hormone responsiveness associated with point mutations in the thyroid hormone receptor-b gene.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dextrothyroxine crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether dextrothyroxine enters human breast milk.

Pregnancy

. Dezocine is a synthetic opioid agonist-antagonist. There is no published experience with dezocine during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dezocine crosses the human placenta. Evidence of rodent teratogenicity is noted in the manufacturer?s information, but not detailed. 281

Breastfeeding

There is no published experience in nursing women. It is unknown whether dezocine enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of diatrizoate in pregnant women. Diatrizoate is a contrast agent frequently used to study bladder structure or function and fallopian tube patency, and in the past for a variety of fetal imaging studies.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether diatrizoate crosses the human placenta. Postnatally, diatrizoate is used diagnostically to distinguish NEC from microcolon of prematurity. Rodent teratogenicity studies have not been performed.

Breastfeeding

A single report suggests that a small amount of diatrizoate may be excreted into human breast milk. However, considering the 282 indication and dosing, one-time diatrizoate use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. There are no adequate reports or well-controlled studies of diazepam in pregnant women. It is a beneficial adjunct to IV fluids and vitamins for the treatment of 1st trimester hyperemesis. Diazepam was previously used for prophylaxis and treatment of eclamptic convulsions, but proved less effective than magnesium sulfate.

Pregnancy

may unmask a preexisting potential for chorea (chorea gravidarum), and benzodiazepines may aid chorea control. Diazepam is a useful antianxietal in women undergoing fetal therapy procedures. Flumazenil (a specific benzodiazepine receptor antagonist) is indicated for complete or partial reversal of the sedative effects, or treatment of a benzodiazepine overdose.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Diazepam rapidly crosses the human placenta, with the F:M ratio approaching unity within 15min of maternal injection and exceeding the maternal level within several hours of administration during labor. Decreased fetal movement frequently accompanies IV administration. Several studies that suggested an increased risk of fetal malformation when diazepam is used during the 1st trimester have not been confirmed subsequently. Postnatal follow-up until age 4y is likewise reassuring, revealing no adverse effects on neurodevelopment. Prolonged CNS depression may occur in neonates, apparently due to their inability to metabolize diazepam. The shortest course and the lowest dose should be used when indicated during pregnancy. Some newborns exposed antenatally exhibit either the floppy infant syndrome or marked neonatal withdrawal symptoms. Symptoms vary from mild sedation, hypotonia, and reluctance to suck to apneic spells, cyanosis, and impaired metabolic responses to cold stress. Such symptoms may persist for hours to months after birth. Rodent studies suggest an increased incidence of fetal malformations (skeletal defects) when administered at much higher doses than ones used clinically. Further, a large body of rodent behavioral studies reveals behavioral alterations that persist into adulthood.

Breastfeeding

Diazepam is excreted into human breast milk to a limited degree. The maximum neonatal exposure is estimated at 3% of the maternal dose. Problems may arise if the neonate is premature, or the maternal dose particularly high. Neonatal lethargy, sedation, and weight loss have been reported, but their attribution to diazepam is not always clear.

Pregnancy

. The mechanism of action of diazoxide remains unclear. It inhibits the production of IL-10 and the proinflammatory cytokines TNF-a and IL-6 by placentas and peripheral blood mononuclear cells. The choice of antihypertensive depends in part on physician experience, and in part on what is known about adverse maternal and fetal Side effects include arrhythmias, seizures, MI, hyperglycemia, hypotension, N/V, weakness, and CHF.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Diazoxide crosses the human placenta, though the kinetics remain to be elucidated. Rodent studies are generally reassuring, revealing no evidence of teratogenicity, though IUGR is seen at the highest doses. Breastfeeding There is no published experience in nursing women. It is unknown whether diazoxide enters human breast milk.

Pregnancy

. There is no published experience with dichlorphenamide during pregnancy. Dichlorphenamide should be used cautiously as it may produce brisk diuresis followed by hypokalemia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dichlorphenamide crosses the human placenta. Rodent studies reveal skeletal anomalies at high doses.

Breastfeeding

There is no published experience in nursing women. It is unknown whether dichlorphenamide enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Diclofenac is a short-acting NSAID with antipyretic, anti-inflammatory, and analgesic properties. It is useful for the relief of ureteral colic or postsurgical pain during pregnancy, or episiotomy after delivery. In several studies, diclofenac had a morphine-sparing effect. While rodent studies reveal very high doses of some NSAIDs are associated with dystocia and prolongation of pregnancy, similar studies in humans are missing for diclofenac. Cyclooxygenase inhibitors such as diclofenac may modulate the quantity and degradation of collagen in the rat cervix. Diclofenac does not interfere with cervical ripening induced by misoprostol. Like other NSAIDs, diclofenac alters renal function to decrease free water clearance and increases the toxicity of certain drugs such as digoxin. Administration at the time of egg collection in women undergoing IVF does not appear to affect implantation or

Pregnancy

rates, while it could be effective in reducing discomfort and pain associated with oocyte retrieval. NOTE: with caution, may be combined with misoprostol (Arthrotec).

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Diclofenac rapidly crosses the human placenta even in the 1st trimester, yielding an F:M ratio approximating unity. Premature closure of the ductus arteriosus is reported. Rodent studies are generally reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. High doses were associated with fetal toxicity. In one recent report, the administration of diclofenac to the ovine fetus blunted the normal increase in cerebral blood flow following a hypoxic episode. While it is unknown whether this same response occurs in association with other NSAIDs or in the human, it suggests the need for caution administering NSAIDs to pregnant women when labor is imminent.

Breastfeeding

There are no adequate reports or well-controlled studies of diclofenac in nursing women. Most NSAIDs enter human milk to some extent. The chemical structure and preliminary study suggest passage should be low and occasional use is without clinically significant risk. Ibuprofen is generally preferred for Breastfeeding women.

Pregnancy

. There are no adequate reports or well-controlled studies of dicloxacillin in pregnant women. Dicloxacillin is a penicillinase- resistant, acid-resistant semisynthetic broad-spectrum penicillin. It is an excellent drug for the treatment of postpartum mastitis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Dicloxacillin crosses the human placenta but the fetal concentrations are relatively low, perhaps because of the high degree of maternal protein binding. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether dicloxacillin enters human breast milk. The extensive clinical experience with its use for mastitis is reassuring. Other penicillin agents are excreted into human breast milk, but are generally considered safe.

Pregnancy

. There are no adequate reports or well-controlled studies of dicyclomine in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dicyclomine crosses the human placenta. Epidemiologic studies are reassuring. Dicyclomine was a component of Bendectin, a popular but no longer marketed drug used to treat N/V during pregnancy. It initially consisted of doxylamine, dicyclomine, and pyridoxine; dicyclomine was dropped from the formulation in 1976. Bendectin was ultimately discontinued in 1983 after an onslaught of lawsuits suggesting it caused congenital malformations. Subsequent studies revealed no difference in the prevalence of birth defects between mothers who had taken Bendectin during the 1st trimester and those who had not. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. Dicyclomine is excreted in human milk. As there are case reports noting severe respiratory symptoms in neonates directly receiving dicyclomine, it is generally considered incompatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of didanosine in pregnant women. Human pharmacokinetic studies suggest maternal plasma clearance after IV administration is significantly greater antepartum than postpartum. Clearance during

Pregnancy

is unaltered after PO administration. Didanosine is no more effective than zidovudine as monotherapy. HIV patients with <400 viral copies/ml respond faster (2 consecutive viral loads <400 copies/ml) and maintain that response for 4y when given a multiregimen treatment including didanosine, stavudine, and nelfinavir compared to lamivudine, zidovudine, and nelfinavir. Resistant strains are known. Didanosine is a cause of diabetes mellitus. Blood glucose levels should be monitored frequently, especially when didanosine is combined with other drugs such as pentamidine and dapsone that cause hyperglycemia. Didanosine does not cure HIV, nor 293 does it reduce the risk of HIV transmission by sexual contact or blood contamination. Fatal lactic acidosis has been reported in pregnant women who have received a combination of didanosine and stavudine. The long-term effects of didanosine on both treated women and neonates are presently unknown.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Didanosine rapidly crosses the isolated human placenta, and efficiently crosses in vivo the macaque placenta. It is estimated the fetal levels would be therapeutic. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Didanosine does cross the rodent placenta.

Breastfeeding

There is no published experience in nursing women. It is unknown whether didanosine enters human breast milk. It is generally recommended that, wherever possible, HIV-infected women not breastfeed to avoid the risk of HIV transmission to the neonate.

Pregnancy

. Dienestrol is a synthetic, nonsteroidal estrogen suitable for intravaginal use. It is also an oxidative metabolic product of diethylstilbestrol. Estrogen compounds are contraindicated during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dienestrol crosses the human placenta. The genital tract has the ability to metabolize dienestrol. Estrogens are contraindicated during pregnancy.

Breastfeeding

There is no published experience in nursing women. It is unknown whether dienestrol enters human breast milk. Estrogens are usually considered incompatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of diethylpropion in pregnant women. The published experience consists of isolated case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether diethylpropion crosses the human placenta. Neonatal withdrawal has been described in neonates delivered of women who used diethylpropion during pregnancy. There is a single case report of sacral agenesis associated with multiple anomalies of the lower limb in a woman taking diethylpropion during the first month of pregnancy. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Diethylpropion is excreted into human breast milk, though the kinetics remain to be elucidated.

Pregnancy

. Diethylstilbestrol was administered to approximately 3 million pregnant women in the US and in thebetween 1947 and 1975. There was an increased risk of mammary carcinomas in exposed women.

Pregnancy

does not appear to influence adversely the tumor characteristics or prognosis of patients who have developed these malignancies.

Fetal Health

There are no adequate reports or well-controlled studies of diethylstilbestrol in human fetuses. It or a metabolite presumably crosses the human placenta. Diethylstilbestrol-exposed daughters frequently have developmental disorders of the cervix and corpus uteri (hypoplasia of the uterine cavity, uterine corpus, and cervix; T-shaped uterine cavity; constrictions of the uterine cavity; and bilateral hydrosalpinges). They have an increased risk of spontaneous abortion, ectopic pregnancy, infertility, possibly cervical incompetence and both cervical and vaginal carcinomas at a young age. Spontaneous uterine rupture at term has also been described. An increased risk of hypospadias in the sons exposed to DES in utero was reported. Rodent experiments reveal that diethylstilbestrol increases the incidence of genital tumors in not only 2nd-generation but also 3rd-generation animals. However, recent studies report no increased risk of lower genital tract abnormalities in 3rd-generation women.

Breastfeeding

Estrogens are contraindicated for lactation suppression. Diethylstilbestrol does not effectively suppress lactation.

Pregnancy

. Diflunisal is an NSAID with anti-inflammatory, antipyretic, and analgesic properties. Similar to many NSAIDs, it inhibits platelet aggregation. There are no adequate reports of diflunisal in pregnant women. Diflunisal is superior to aspirin for the relief of postepisiotomy pain.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether diflunisal crosses the human placenta. Treated Cynomolgus monkeys experience no increased rates of abortion, IUGR, or malformation. Rodent studies reveal embryotoxicity and teratogenicity (skeletal malformations) in doses 1-8the MRHD. In the human fetus, 298 other NSAIDs can cause in the 3rd trimester constriction of the ductus arteriosus, followed by tricuspid incompetence and pulmonary hypertension. Platelet dysfunction, intracranial bleeding, or renal dysfunction may result in permanent renal failure, oligohydramnios, or necrotizing enterocolitis.

Breastfeeding

There is no published experience in nursing women. Diflunisal is excreted into human milk, achieving an M:P ratio <0.07. Considering the indications and dosing, occasional diflunisal use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. There are no adequate reports or well-controlled studies of digitoxin in pregnant women. Digitoxin is a crystalline-pure cardiac glycoside obtained from Digitalis purpurea and has pharmacologic action identical to that of digitalis. Excretion is slow (14-21d). Serum levels should be monitored periodically during pregnancy. Pregnant women receiving the usual dose of 0.25mg tend to have subnormal levels and may require a small increase during the 3rd trimester.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Digoxin and presumably digitoxin cross the healthy human placenta, reaching F:M ratios approximating 0.8. However, the human placenta is rich in digoxin receptors, and placental binding increased and transfer decreased when there is hydrops. Fetal bradycardia is reported. Studies are compromised by tests that failed to differentiate between digoxin and endogenous digoxin-like substances. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether digitoxin enters human breast milk. Endogenous digoxin- like substances are normal components of breast milk.

Pregnancy

. There is a long clinical experience with digoxin during

Pregnancy

and the puerperium for the treatment of benign arrhythmias and cardiomyopathy. A full CV evaluation is recommended prior to its initiation. Potential stimulants, such as smoking, caffeine, and alcohol should be eliminated. Although no antiarrhythmic drug is completely safe during pregnancy, most are well tolerated and add relatively little risk. Drug therapy should be avoided during the 1st trimester and drugs with the best safety record used as first-line therapy. Women with peripartal cardiomyopathy who have persistently abnormal ventricular function must be continuously treated with digoxin, diuretics, and anticoagulation, and have the same relatively poor prognosis as patients with dilated cardiomyopathy. Heart transplantation may be necessary for survival.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Digoxin crosses the placenta, with a typical F:M ratio ranging from 0.6 to 0.8. There are, however, a high concentration of placental digoxin receptors and significant back- transport of digoxin by placental P-glycoprotein. Digoxin is generally considered first-line therapy for the treatment of fetal SVT in the absence of hydrops. Treatment is aimed initially at slowing the ventricular response rate and ultimately conversion to sinus rhythm. However, there are no trials confirming that conversion reflects therapeutic efficacy or disease natural history. After adequate maternal digitalization, conversion to normal sinus rhythm should occur within 72h; reported successes often occur after weeks. Certainly, the addition of a second agent would be desirable if there is no response. The fetal response is worse if tricuspid regurgitation is already present. Placental transport is dramatically reduced when there is hydrops, and this appears inversely proportional to the umbilical venous pressure. In this instance, many fetal medicine specialists consider flecainide a drug of choice. Direct fetal digoxin administration (IM) can be successful after more traditional intensive trials of transplacental therapy with digoxin, verapamil, and procainamide, either separately or in combination, fail. Transplacental digoxin therapy has also been used to improve ionotropy in fetuses with complete heart block. Despite adequate therapy and many times improvement in the fetal status in utero, many fetuses require postnatal pacemaker implantation or heart transplantation. Rodent teratogenicity studies have not been performed. 301

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Digoxin enters human breast milk in low concentration, achieving an M:P ratio approximating 0.7. As a result, the digoxin level of the breastfed neonate would be subtherapeutic. Endogenous digoxin-like substances are a normal component of breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of dihydroergotamine in pregnant women. It possesses oxytocic properties and was used in several older trials to assist with the induction of labor. It was also used occasionally during

Pregnancy

for the treatment of ??low?? BP. Neither of the last 303 two are indications. Dihydroergotamine is effective for the treatment of menstrual migraine.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dihydroergotamine crosses the human placenta. In one series, women with ??low?? BP were treated for 1w and the fetal umbilical artery S/D ratio increased 22%, thus suggesting placental transfer. In guinea pigs, chronic administration of dihydroergotamine is associated with IUGR suggesting decreased placental blood flow.

Breastfeeding

There is no published experience in nursing women. It is unknown whether dihydroergotamine enters human breast milk. It is known that ergots inhibit prolactin, and that ergotamine is excreted into human breast milk and can have adverse effects on the breastfed neonate. It would be reasonable to stop Breastfeeding until the headache has resolved.

Pregnancy

. There are no adequate reports or well-controlled studies of dihydrotachysterol (vitamin D) in pregnant women, though it is part of most prenatal vitamin preparations. Dihydrotachysterol and calcitriol are both effective for the management of hypoparathyroidism during pregnancy. The dose required typically needs to be readjusted up during the latter half of gestation. The dose of calcitriol should be reduced during lactation.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dihydrotachysterol crosses the human placenta, nor is it known whether dihydrotachysterol increases fetal calcium. However, fetal supravalvular aortic stenosis may be associated with hypercalcemia secondarily to hypervitaminosis D, and hypercalcemia can occur during treatment with dihydrotachysterol. Rodent teratogenicity studies reveal similar abnormalities.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. While dihydrotachysterol increases the amount of calcium in breast milk, hypercalcemia is not seen in breastfed neonates. It is considered unlikely to have a clinically significant effect on the Breastfeeding neonate.

Pregnancy

. There are no adequate reports or well-controlled studies of diltiazem in pregnant women. Clearance is unaltered during rabbit pregnancy. Diltiazem is used for the treatment of acute cardiac rhythm emergencies. In vitro and in vivo studies demonstrated effective inhibition of myometrial contractions and vasodilation of arteries collected from normal and preeclamptic women. Oral diltiazem has no advantage over nifedipine as a tocolytic agent. The CV alterations following either drug appear minimal in normotensive, pregnant women. Volume loading and a supine position further reduces the risk of an adverse CV reaction. Case reports document successful treatment of maternal angina secondary to coronary spasm. Recently, a relationship 306 between oral erythromycin and sudden cardiac death was reported in patients also receiving strong inhibitors of CYP3A such as nitroimidazole antifungal agents, diltiazem, verapamil, and troleandomycin; each doubles, at least, the AUC for a CYP3A substrate.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether diltiazem crosses the human placenta. It does rapidly cross the rabbit placenta. Rodent studies suggest an increased incidence of skeletal and aortic arch malformations in some species at doses of diltiazem administered in multiples of the MRHD. Another study of rabbits concluded that chronic in utero exposure altered postnatal metabolism.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Diltiazem enters human milk and may reach maternal serum levels. Though generally considered safe for Breastfeeding women, it may be wise to consider another calcium channel blocker.

Pregnancy

. There are no adequate reports or well-controlled studies of dimenhydrinate in pregnant women. It is a popular agent in many locales for the relief of N/V during pregnancy, though the practice is unsupported by a single clinical trial. Both dimenhydrinate and diphenhydramine are considered treatment options for severe migraine headache during pregnancy. Caution is warranted since several investigators report an increase in uterine activity associated with dimenhydrinate.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dimenhydrinate crosses the human placenta. There is no indication that dimenhydrinate increases the risk of fetal abnormalities when given at any stage of pregnancy. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. One recent epidemiologic study actually observed a lower prevalence of obstructive uropathy in exposed infants.

Breastfeeding

There is no adequate published experience in nursing women. Dimenhydrinate is excreted in small quantities into human breast milk, though the kinetics remain to be elucidated. A long clinical experience is reassuring.

Pregnancy

. Dinoprostone is the naturally occurring PGE2. It is effective when administered by oral, vaginal, or intracervical routes for cervical ripening preceding either vaginal delivery or

Pregnancy

termination. Efficacy is maintained after membrane rupture. Complications include tachysystole and uterine rupture. Outpatient use has been advocated, but there is no dose that assures the absence of tachysystole. The risk of the latter is especially great in women with a prior cesarean section. Two recent randomized trials compared dinoprostone to misoprostol for the induction of labor in women including those at high risk for fetal distress. Misoprostol and dinoprostone are equally safe for the induction of labor. However, misoprostol is more efficient, may be associated with a lower cesarean delivery rate, and is significantly cheaper. Dinoprostone reduces the risk of postpartum hemorrhage in high-risk patients. It has also been used to treat atony. Hypertension and anaphylaxis have been reported on occasion. The safety profile of dinoprostone is good; it has been used successfully in women with a wide range of medical complications.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dinoprostone crosses the human placenta. Any effect on the fetus appears to reflect complications of uterine activity, as cervical priming has no effect 310 on fetal blood flows. Rodent studies reveal embryotoxicity and an increased prevalence of skeletal anomalies when given during organogenesis.

Breastfeeding

There is no published experience in nursing women. It is unknown whether dinoprostone enters human breast milk. However, considering the indication and dosing, dinoprostone use is unlikely to pose a clinically significant risk to the Breastfeeding neonate. PGE2is naturally excreted into breast milk and has been reported as a cause of neonatal diarrhea.

Pregnancy

. There are no adequate reports or well-controlled studies of diphenhydramine in pregnant women. It has a long history of use in obstetrics. Diphenhydramine is a useful adjunct for women who have allergic reactions to local anesthesia, laminaria, and serum albumin, or for the treatment of severe migraine headaches.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Though diphenhydramine crosses the human placenta, the kinetics remain to be elucidated. There is no evidence of increased fetal risk if administered during any stage of pregnancy. Diphenhydramine may cause neonatal depression if administered during labor. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether diphenhydramine enters human breast milk. Irritability is the most common adverse reaction reported in the newborns of women using antihistamines while breastfeeding. 312

Pregnancy

. Thromboembolus is a major complication of mechanical heart valves. The risk is greatly reduced but not eliminated by regimens of anticoagulation with warfarin or therapeutic heparin in addition to an antiplatelet agent. Warfarin is relatively contraindicated during pregnancy. The regimen of dipyridamole, 313 aspirin, and ticlopidine also appears to be effective prophylaxis. The effect on platelet function persists for about 72h after discontinuing therapy, but is not associated with a change in the bleeding time. Because preeclampsia is associated with a subclinical DIC state, and IUGR with placental thrombosis, a number of studies have examined the role of dipyridamole to reduce their incidence. For the most part, dipyridamole adds little to the beneficial effects of 81mg of aspirin for these indications. Dipyridamole has also been used for the treatment of essential thrombocythemia during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dipyridamole crosses the human placenta. The addition of dipyridamole to aspirin does not enhance the beneficial effect of aspirin on preventing IUGR. Dipyridamole use is associated with decreased Doppler measured flow resistance in the umbilical artery. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no adequate published experience in nursing women. Dipyridamole enters human milk, though the kinetics remain to be elucidated. There is no evidence to suggest a neonatal effect that would preclude breastfeeding. It has been used to treat respiratory difficulties in newborns with congenital diaphragmatic hernia.

Pregnancy

. There is no published experience with dirithromycin during pregnancy. Dirithromycin is converted in the intestine to the microbiologically active erythromycylamine. Dirithromycin is comparable in efficacy to erythromycin for the treatment of skin and soft tissue infections with significantly less nausea. Once-daily dosing aids compliance.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dirithromycin crosses the human placenta. Other macrolides cross the placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. Very high doses were associated with IUGR.

Breastfeeding

There is no published experience in nursing women. It is unknown whether dirithromycin enters human breast milk. It is excreted into rodent milk. Other macrolides are considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of disopyramide in pregnant women.

Pregnancy

alters the percentage of free drug circulating in the plasma. Treatment of a cardiac arrhythmia with disopyramide during

Pregnancy

is complicated by reported risks of hemorrhage or hypotension or uterine contractions leading to fetal distress. Patients should be monitored intensively to detect such complications. Disopyramide is actually superior to placebo for the induction of labor.

Fetal Health

There are no adequate reports or well-controlled studies of disopyramide in human fetuses. It crosses the human placenta, achieving an F:M ratio approximating 0.26 for disopyramide, and 0.43 for its main metabolite, N-monodesalkyl disopyramide. Rodent studies are reassuring, revealing no evidence of teratogenicity despite doses higher than those used clinically. The highest doses were associated with embryotoxicity and IUGR.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Though disopyramide is concentrated in human breast milk over maternal plasma after oral administration, the unsupplemented newborn would ingest <2mg/kg. Not 316 surprisingly, disopyramide is at or below the level of detection in the neonate.

Pregnancy

. There are no adequate reports or well-controlled studies of disulfiram in pregnant women. Disulfiram is a deterrent to alcohol consumption in patients with a history of alcohol abuse. Its use is increasingly more common in reproductive-age women. 317 The safety of disulfiram during

Pregnancy

is not established. The published literature consists mostly of case reports and small series.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether disulfiram crosses the human placenta. There are several case reports of limb abnormalities in alcoholic women treated with disulfiram during pregnancy. In vitro, disulfiram is embryotoxic, affecting both DNA synthesis and morphologic development.

Breastfeeding

There is no published experience in nursing women. It is unknown whether disulfiram enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of divalproex in pregnant women. Divalproex is a stabilized form of valproic acid. It disassociates into valproate in the GI tract. While the metabolism of valproate is unaltered by pregnancy, clearance is increased primarily because of decreased binding. It is suggested the drug be taken in divided doses to avoid high peaks (see valproic acid). Among patients treated for a bipolar disorder, the risk of suicide attempt is higher during treatment with divalproex than it is with lithium. However, divalproex for the prevention of postpartum episodes of bipolar disorder does not appear more effective than monitoring without drug. Valproate seems to reduce the induction of lamotrigine metabolism associated with

Pregnancy

or use of contraceptives. Monitoring of anticonvulsant drug levels with appropriate dose adjustments is warranted throughout pregnancy, and vitamin K (10mg/d) should be given in the last month of gestation, particularly when CYP enzyme?inducing agents are being used.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Valproate and its metabolites cross the placenta, perhaps by a proton-linked transport system, and are concentrated in fetal plasma at least in part because of increased protein binding. The F:M ratio exceeds unity. Valproate is a human teratogen. Valproic acid has been associated with a variety of major and minor malformations, including a 20-fold increase in NTDs, cleft lip and palate, CV abnormalities, GU defects, developmental delay, endocrinologic disorders, limb defects, and autism. Divalproex monotherapy during the 1st trimester increases the risk of a fetal NTD by about 10?, or to a prevalence of 1-2%. This association likely reflects pharmacogenetics since preconception maternal folate supplementation does not necessarily reduce the risk of recurrence in subsequent pregnancies. Other associated malformations involve the CV system and the limbs. Its combination with other anticonvulsants increases the risks of malformation. In one small but population-based study, all children exposed to valproate had minor, and some of them major, cognitive or neurologic problems. The placenta is not a depot for valproic acid. It would appear that there are more adverse outcomes in pregnancies with in utero valproate exposure vs. the other antiepileptic drugs. Other agents should be used whenever possible. For women who fail other antiepileptic drug therapy and require valproate, the dose should be limited if possible. As for most psychotropic drugs, monotherapy and the lowest effective quantity given in divided doses to minimize the peaks can minimize the risks. (See Valproic acid.)

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only small amounts of valproate (1-10%) enter human breast milk, and its serum concentration in breastfed neonates is subclinical. (See Valproic acid.) 319

Pregnancy

. There are no adequate reports or well-controlled studies of dobutamine in pregnant women. Dobutamine is a direct-acting b-adrenergic ionotropic agent producing a pressor effect with less chronotropy than the b-adrenergic agents, plus some degree of vasodilation (e.g., pulmonary vascular resistance) but no dopaminergic renal effects. Dobutamine is recommended for ionotropic support of women with cardiac decompensation during pregnancy. It is used to improve ventricular function in 321 women with idiopathic dilated cardiomyopathy. Dobutamine can also induce a modest but unsustained increase in cardiac output in patients with idiopathic pulmonary hypertension. The diagnosis of peripartal cardiomyopathy is limited to women with CHF and decreased LV systolic function during the last month of

Pregnancy

or within 5mo of delivery. Women whose ventricular function is normal at rest and exercise may have their dobutamine tapered and ultimately discontinued after 6-12mo. The dobutamine challenge test is used to assess ventricular function in women with a history of peripartal cardiomyopathy who have regained normal resting LV size and performance. Digoxin is recommended prior to dobutamine when treatment is necessary for atrial fibrillation.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Dobutamine crosses the human placenta, though the kinetics remain to be elucidated. Dobutamine has been used in twin-twin transfusion syndrome with possible benefit. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether dobutamine enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of docetaxel in pregnant women. There are now several case reports of its use during

Pregnancy

with reassuring results.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether docetaxel crosses the human placenta. While there is no evidence of teratogenicity, rodent studies reveal clear evidence of both embryo and fetal toxicity at doses far below those used in humans.

Breastfeeding

There is no published experience in nursing women. It is unknown whether docetaxel enters human breast milk. However, it is generally considered incompatible with Breastfeeding in light of its pharmacologic mechanism.

Pregnancy

. While there are no adequate reports or well-controlled studies of docusate in pregnant women, there is a long clinical experience with virtually no reported complications. Docusate is frequently used postpartum to avoid constipation in women who have had a repaired episiotomy. It may rarely potentiate the hepatotoxicity of other drugs.

Fetal Health

Docusate is not absorbed systemically and thus does not cross the placenta. A three-generational rodent study failed to identify any adverse effects on reproduction. There are reports of neonatal hypomagnesemia after maternal abuse of stool softeners.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Docusate is not absorbed systemically and thus will not enter human breast milk.

Pregnancy

. There is no published experience with dofetilide during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dofetilide crosses the human placenta. Rodent studies reveal that dofetilide produces a spectrum of defects similar to phenytoin, including cardiac, digital, and oral facial clefting malformations, possibly by blocking potassium channels.

Breastfeeding

There is no published experience in nursing women. It is unknown whether dofetilide enters human breast milk.

Pregnancy

. There is no published experience with dolasetron during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dolasetron crosses the placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether dolasetron enters human breast milk.

Pregnancy

. Donepezil is believed to enhance cholinergic function by increasing ACh concentration in the intact cholinergic nerves, keeping them functionally intact. Further, donepezil potentiates activity of the NMDA system even at low therapeutic concentrations (0.01-1mcM). This action together with cholinesterase inhibition could contribute to the improvement of learning, memory, and cognition in patients with Alzheimer?s disease. There is no evidence that donepezil alters the course of the underlying disease. It is metabolized by CYP isozymes 2D6 and 3A4 and undergoes glucuronidation. Neither gender nor race appears to alter clearance, though it is prolonged by cirrhosis. There is no published experience with donepezil during pregnancy.

Fetal Health

There is no published experience in human pregnancy. It is unknown whether donepezil crosses the human placenta. Rodent studies are for the most part reassuring, revealing no evidence of teratogenicity at up to 18the MRHD. At 8the MRHD, the stillbirth rate was slightly increased in rats.

Breastfeeding

There is no published experience in nursing women. It is unknown whether donepezil enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of dopamine in pregnant women. Dopamine is a natural catecholamine that produces both positive chronotropic and inotropic effects. Several investigators have applied its vasodilating properties to the treatment of preeclamptic hypertension. A low- dose infusion of dopamine aids the management of acute renal failure caused by preeclampsia. A treatment program of IV fluids, furosemide, and/or dopamine has been suggested for preeclamptic women with anuria (output <100ml/24h). If unsuccessful, early dialysis should be considered. The evidence for the use of prophylactic medical interventions (e.g., the use of loop diuretics, mannitol, and low-dose dopamine), is poor. Studies in monkeys report both increased and decreased uterine blood flow depending on dose.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. There are specific dopamine receptors on the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Maternal toxicity occurred and was associated with decreased neonatal survival.

Breastfeeding

There is no published experience in nursing women. It is unknown whether dopamine enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of doxazosin in pregnant women. It is similar to atenolol.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether doxazosin crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether doxazosin enters human breast milk. It is concentrated in rodent milk. Similar agents are generally considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of doxepin in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether doxepin crosses the human placenta.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. While only small amounts of doxepin and its active metabolite enter breast milk, one report described apnea and drowsiness though the neonatal plasma doxepin was just into the detectable range. Caution is suggested.

Pregnancy

. There are no adequate reports or well-controlled studies of doxorubicin in pregnant women. Irreversible myocardial toxicity may occur during or months after therapy. ACEIs and dexrazoxane offer cardioprotection. Women with breast cancer diagnosed during

Pregnancy

are frequently treated during the 1st trimester of

Pregnancy

with a complex regimen including fluorouracil, doxorubicin, and cyclophosphamide. Women with Hodgkin?s lymphoma who survived without recurrence ?3y and who attempt

Pregnancy

after combination chemotherapy including doxorubicin do not experience significant subfertility.

Fetal Health

Though there are no adequate reports or well-controlled studies in human fetuses, there are numerous uncontrolled series and case reports whose interpretations are complicated by the fact that doxorubicin is often given with other agents. There is no firm evidence of teratogenicity or perinatal myocardial dysfunction in fetuses of women treated with doxorubicin. Women treated during the 2nd and 3rd trimesters of

Pregnancy

experience little increase in the rate of complication during labor and delivery, and their neonates do well. There is essentially no long-term follow-up of exposed fetuses. Doxorubicin is associated with a series of anomalies in rats similar to VATER?esophageal atresia, tracheoesophageal fistula, and cloacal and urogenital anomalies.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Doxorubicin is concentrated in human breast milk, achieving maximum M:P ratios approximating 4.4. However, the maximum concentration of active drug approximates 0.24mg/L. Thus, the amount ingested by the Breastfeeding neonate would be insignificant.

Pregnancy

. Doxycycline is synthetically derived from oxytetracycline (see Tetracycline).

Fetal Health

Use of tetracyclines during tooth development (3rd trimester, infancy, and in children <8y) may cause permanent discoloration of the teeth (see Tetracycline). 335

Breastfeeding

See Tetracycline.

Pregnancy

. There are no adequate reports or well-controlled studies of dronabinol in pregnant women. Several publications suggest a relationship between cannabis use and head and neck cancers in a dose-response manner for frequency and duration of use. Interaction was observed with cigarette smoking and alcohol use.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dronabinol crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. 336

Breastfeeding

There is no published experience in nursing women. It is unknown whether dronabinol enters human breast milk. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. There are no adequate reports or well-controlled studies of droperidol in pregnant women. It has been used in emergency 337 rooms for the acute management of migraine headache with success similar to meperidine. Droperidol, propofol, and alizapride, in decreasing order of effectiveness for the doses used in this study, reduced the incidence of pruritus induced by the use of intrathecal morphine. In addition, droperidol reduces N/V after epidural morphine similar in efficacy to dexamethasone. The addition of metoclopramide appears to enhance its efficacy. In one study, it was inferior to granisetron after cesarean section. There is a black box warning currently issued by the FDA based on reports of prolonged QT?associated dysrhythmia. However, the dozens of cases reported to the FDA were in fact multiple reports of 3 cases.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether droperidol crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Neonatal mortality was increased perhaps because of maternal neglect.

Breastfeeding

There is no published experience in nursing women. It is unknown whether droperidol enters human breast milk. However, considering the indications, its short-term use is unlikely to pose a significant risk to the Breastfeeding neonate.

Pregnancy

. Econazole has been used for the treatment of Candida vaginitis with success somewhat inferior to clotrimazole. Systemic absorption of econazole is extremely low. There are no adequate reports or well-controlled studies of econazole in pregnant women. However, it was effective in vitro using samples obtained from pregnant women. Econazole prolongs

Pregnancy

in rats when given orally.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether econazole crosses the human placenta. One epidemiologic study of women using vaginally administered econazole is reassuring. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Embryotoxic effects were noted in rodents after oral administration of 10-40the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether econazole enters human breast milk. It is present in rodent breast milk after high oral doses. Considering the indication, dosing, and route, it seems unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Edrophonium is a short- and rapid-acting cholinergic drug. There are no adequate reports or well-controlled studies of edrophonium in pregnant women. Older literature suggests anticholinesterases may trigger preterm labor.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether edrophonium crosses the human placenta; the chemical structure suggests it will not. There are no reports of either fetal toxicity or teratogenicity. Rodent teratogenicity studies apparently have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether edrophonium enters human breast milk. The chemical structure suggests it will not be excreted into the breast milk. Considering the indication, one-time edrophonium use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. There are no adequate reports or well-controlled studies of efavirenz in pregnant women. However, there are several case series of HIV-infected women who have conceived while taking efavirenz. It is common practice to switch women on efavirenz to another NNRTI. The vast majority of these pregnancies are unintended, stressing the importance of contraceptive counseling. Hepatotoxicity may be more common during pregnancy. Perhaps the most relevant consideration when initiating a pregnant woman on an NNRTI is whether normally tolerated Side effects include Stevens-Johnson syndrome, dermatitis, erythema multiforme, rash, drowsiness, insomnia, abnormal dreams, hyperlipidemia, diarrhea, N/V, fever, and hepatic dysfunction.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Efavirenz crosses the placenta, achieving an F:M ratio approximating unity. Its use has been associated with CNS malformations in monkey fetuses at doses that approximate those in humans, and with NTDs in exposed human fetuses. These studies led to a reclassification of the drug to category D. Rodent studies reveal an increased frequency of reabsorptions. Breastfeeding Efavirenz enters human breast milk. In one study with a mean efavirenz maternal plasma concentration of 6.6 mg/L, the milk concentration was 3.5 mg/L and the infant plasma level was 0.9 mg/L.

Pregnancy

. Migraine is a paroxysmal disorder with attacks of headache, N/V, photo- and phonophobia, and malaise. There is no published experience with eletriptan during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether eletriptan crosses the human placenta. In mice and rabbits, eletriptan at 6-12the MRHD during organogenesis is associated with IUGR and skeletal abnormalities.

Breastfeeding

According to the manufacturer, eletriptan is excreted in human breast milk. The mean total amount of eletriptan in breast milk after a single 80mg dose over 24h approximated 0.02% of the administered dose. The M:P ratio was 1:4, but showed great variability. The resulting eletriptan concentration-time profile is similar to plasma, with very low concentrations of drug present in the milk 18-24h after ingestion (mean, 1.7 ng/ml).

Pregnancy

. There are no adequate reports or well-controlled studies of enalapril in pregnant women. It is generally well tolerated, and

Pregnancy

does not alter dosing. However, enalapril should be discontinued immediately when discovered during

Pregnancy

and replaced with another suitable hypotensive agent to prevent or minimize the fetal risks.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Enalapril crosses the human placenta, but does not equilibrate, even after 6h, at least in the isolated perfused model. Relative to laboratory-tested species, the human fetus has higher vulnerability to enalapril and other ACEIs, exhibiting a syndrome not seen in experimental animals because humans develop these systems prior to calvarial ossification at the end of 1st trimester. Exposure to agents that interfere with angiotensin actions are associated with cranial hypoplasia, anuria, reversible or irreversible renal failure, death, oligohydramnios, prematurity, IUGR, and patent ductus arteriosus, even in the 1st trimester. Longterm renal disease is reported in survivors. Enalapril produces fetal hypotension in rhesus macaques. 344

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Trace amounts of enalapril are detected in breast milk, though the kinetics remain to be elucidated. Until further study, the infant should be monitored for possible adverse effects, the drug given at the lowest effective dose, and Breastfeeding avoided at times of peak drug levels if

Pregnancy

. Encainide was voluntarily removed from the market in 1991 but remains available for patients with certain life-threatening arrhythmias. There are no adequate reports or well-controlled studies of encainide in pregnant women. There is only a single case report of encainide use for a maternal arrhythmia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether encainide crosses the human placenta. A related drug, flecainide, does cross the human placenta and reaches therapeutic levels in the fetus. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. Encainide enters human breast milk, though its kinetics remains to be detailed. Flecainide is excreted at low levels and is generally considered safe during breastfeeding.

Pregnancy

. There are no published reports of enoxacin use during pregnancy. It is a broad-spectrum agent with high oral absorption. It is not effective for the treatment of syphilis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether enoxacin crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Adverse effects were associated with maternal toxicity. As a class, the new quinolones do not appear associated with an increased risk of malformation or musculoskeletal problems in humans. Longer follow-up and MRI of the joints may be warranted to exclude subtle cartilage and bone damage. There are no clinically significant musculoskeletal dysfunctions reported in children exposed to other fluoroquinolones in utero.

Breastfeeding

There is no published experience in nursing women. It is unknown whether enoxacin enters human breast milk. It does enter rodent milk, and other quinolone-type drugs are excreted into human breast milk. In some animals, slow elimination of a related agent, ciprofloxacin, results in blood levels out of proportion to the dose ingested. Because of the potential for some quinolones to cause arthropathy in juvenile animals, they should be avoided in pregnant and lactating women until more information is available.

Pregnancy

. The incidence of PE and DVT is higher in pregnant compared to nonpregnant patients, reaching a rate of 0.05-1% in all pregnancies, and as high as 3% after cesarean section.

Pregnancy

increases the clearance of both heparin and low-MW heparinoids such as enoxaparin requiring periodic monitoring throughout

Pregnancy

(anti-Xa activity of 0.20-0.40U/ml for prophylaxis, and 0.4-0.7U/ml for full anticoagulation). The mean maximum dose required to achieve a therapeutic anti-Xa level at 5-6h after injection in one study was 38.1mg every 12h (range 30-75mg every 12h). The mean anti-Xa level was 0.28IU/ml (median 0.3, range 0.05-0.8IU/ml). The risk of osteoporosis is similar to unfractionated heparin, though the risk of thrombocytopenia may be lower. Acute thrombosis should be treated with therapeutic anticoagulation for the remainder of

Pregnancy

and for at least 6w postpartum (a minimum of 3mo total). One as-yet unconfirmed report suggests the addition of enoxaparin to the therapy of women with gestational hypertension may have a beneficial effect on uterine blood flow. Enoxaparin has also been used for prophylaxis during

Pregnancy

in women with thrombophilia or mechanical heart valve or antiphospholipid syndrome. There have been multiple deaths of treated pregnant women with a mechanical heart valve, and the manufacturer specifically discourages its use for this indication. Women treated with LMWHs for prevention of thromboembolic complications are at risk of developing an epidural or spinal hematoma after neuraxial anesthesia. Unlike unfractionated heparin, enoxaparin is not predictably reversed with protamine. Preferably, LMWHs are replaced with unfractionated heparin at 348 36w. Otherwise, patients should be instructed to withhold their next injection once contractions begin, or 12h prior to a planned induction of labor. Enoxaparin should be discontinued 12-24h (depending on daily dose) before placement of neuraxial (epidural or spinal) anesthesia. Enoxaparin should not be (re)instituted until at least 12h after removal of an indwelling epidural catheter.

Fetal Health

Neither unfractionated nor fractionated heparin crosses the human placenta, and thus enoxaparin does not pose a direct risk to the human fetus. Epidemiologic studies are reassuring. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. One investigation found no anti-Xa activity in the breast milk from a single patient. Enoxaparin is unlikely to cross in light of its high MW, and if it does cross and is ingested by the nursing newborn, it is likely to be degraded.

Pregnancy

. There are no adequate reports or well-controlled studies of ephedrine in pregnant women. When abused as a decongestant, ephedrine may exacerbate the hypertension associated with preeclampsia. There is a long clinical experience with the use of ephedrine during labor to treat hypotension associated with neuraxial anesthesia. It is considered the vasopressor of choice unless contraindicated by maternal condition (e.g., coexisting valvular stenosis) and is protective of the uterine circulation, perhaps through release of NO in the placental vessels. But while interventions such as colloids, ephedrine, phenylephrine, or lower leg compression reduce the incidence of hypotension, none has been shown to eliminate the need to treat maternal hypotension during spinal anesthesia for cesarean section. Women with preeclampsia are less likely to experience hypotension at the time of spinal anesthesia, and require significantly less ephedrine when they do.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Ephedrine apparently crosses the placenta, though the kinetics remain to be elucidated. Rodent teratogenicity studies have not been conducted. The long clinical experience with the drug, both in OTC preparations and in the labor suite, is reassuring.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Ephedrine is excreted and concentrated into breast milk, but <1% of the ingested dose is excreted. Thus, it is generally considered safe for Breastfeeding women. However, a single dose of pseudoephedrine reduces 24h milk production by as much as 25%.

Pregnancy

. Epinephrine is commonly used for the relief of severe bronchospasm secondary to allergy. There are no adequate reports or well-controlled studies of epinephrine in pregnant women. Theoretically, it could lead to a decrease in uterine blood flow. Epinephrine in solution with local anesthetic decreases vascular absorption of local anesthetic, intensifying neural blockade and in some cases prolonging the duration of the block. The maternal response may be potentiated by a variety of drugs and by preeclampsia. 351

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Epinephrine apparently rapidly crosses the human placenta, which is rich in catecholamine receptors. It is teratogenic in mice at 25the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether epinephrine enters human breast milk. However, considering the indication, dosing, and its rapid destruction when orally ingested, epinephrine use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. There are no adequate reports or well-controlled studies of epoetin in pregnant women. Case series suggest hypertension may complicate as many as 20% of cases. It is often prescribed for pregnant women under going chronic renal dialysis. Adjuvant epoetin safely enhances the efficacy of iron sucrose in the treatment of gestational iron deficiency anemia resistant to orally 352 administered iron alone. In one case report, it was used successfully to treat a pregnant Jehovah?s Witness with sickle cell disease.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether epoetin crosses the human placenta. It does not cross the isolated placental cotyledon. In the offspring of rats treated with 500U/kg, a diverse group of abnormalities was observed, including delayed ossification. There were no effects below that dose.

Breastfeeding

There is no published experience in nursing women. It is unknown whether synthetic epoetin enters human breast milk, though erythropoietin is a normal component of breast milk.

Pregnancy

. Epoprostenol is prostacyclin. PPH is a rare, progressive condition aggravated by the physiologic changes of pregnancy. Epoprostenol has been used to treat women during

Pregnancy

and in the immediate postpartum period with apparent success. The maternal mortality rate ranges from 30% to 50%.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether epoprostenol crosses the human placenta. A small amount of carbacyclin is transferred across isolated cotyledons from normal placentas. The placenta and fetus synthesize large quantities of prostacyclin. There is no reason to suspect toxicity. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether epoprostenol is excreted into breast milk. However, prostacyclin is a normal component of human breast milk.

Pregnancy

. There is no published human experience with eprosartan during pregnancy. However, extensive experience with other compounds that inhibit aspects of the angiotensin-renin system indicate it should be avoided during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether eprosartan crosses the 354 human placenta. Similar class drugs are known teratogens. While no adverse fetal effects are reported after 1st trimester exposure, later exposure to agents that interfere with angiotensin action is associated with cranial hypoplasia, anuria, reversible or irreversible renal failure, death, oligohydramnios, prematurity, IUGR, and patent ductus arteriosus. This ??ACEI fetopathy?? does not have a counterpart in experimental animals because humans develop these systems prior to calvarial ossification at the end of 1st trimester.

Breastfeeding

There is no published experience in nursing women. It is unknown whether eprosartan enters human breast milk. Eprosartan is excreted into rodent breast milk. Until further study, the infant should be monitored for possible adverse effects, the drug given at the lowest effective dose, and Breastfeeding avoided at times of peak drug levels if

Pregnancy

. The recommended minimal daily requirement of vitamin D is 400U. The safety of larger doses is unknown. Ergocalciferol is a synthetic regulator of calcium. There are few well-controlled studies of ergocalciferol in pregnant women. Oral supplementation of vitamin D deficient women does raise serum 25-hydroxy vitamin D concentrations. There is a long clinical experience of ergocalciferol supplementation during

Pregnancy

and lactation without complications. Meta-analysis suggests supplementation with ergocalciferol reduces the risk of a fall in the elderly by more than 20%.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether ergocalciferol crosses the human placenta. Maternal vitamin D supplementation does not significantly increase the neonatal level. Ergocalciferol or a metabolite crosses the rodent placenta. Hypervitaminosis D has been associated with a syndrome characterized by supravalvular aortic stenosis, elfin facies, and mental retardation. Rare reports in fetal rats suggesting anomalous bone development when administered in high doses with cortisone. Neonates with low vitamin D have low levels of IL-10, a marker for future allergies.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether ergocalciferol enters human breast milk. Vitamin D is a normal component of breast milk, and ergocalciferol has little effect on vitamin D metabolites in human breast milk. It is likely simple supplementation is safe during lactation. However, there is a single case report of a woman given large doses of vitamin D where 25-hydroxycholecalciferol was identified in her breast milk and the neonate developed hypercalcemia.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Ergotamine is a highly active uterine contractile agonist. Inadvertent use may lead to abortion. Epidemiologic study reveals an increased prevalence of preterm birth and IUGR in ergotamine users. Ergotamine produces constriction of both arteries and veins. It causes constriction of peripheral and cranial blood vessels and depresses the central vasomotor centers. The pain of a migraine attack is believed secondary to greatly increased amplitude of pulsations in the cranial arteries, especially the meningeal branches of the external carotid artery. Ergotamine reduces extracranial blood flow, decreases the amplitude of pulsation in the cranial arteries, and decreases hyperperfusion of the territory of the basilar artery. It is effective in controlling up to 70% of acute migraine attacks and is considered specific for the treatment of this headache syndrome. Atropine or antiemetic compounds of the phenothiazine group may relieve the associated N/V. There is a case report of its association with maternal MI following an ergotamine-associated abortion.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether ergotamine crosses the human placenta. While there is no clear evidence it is a teratogen, the severe vasoconstriction associated with toxicity could lead to profound fetal hypoxia and death. It has also been associated with Mo?bius? syndrome.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Ergotamine is excreted into human breast milk. Theoretically, excessive dosing or prolonged administration of ergotamine might inhibit lactation. Though generally considered incompatible with breastfeeding, the only published study found no effect on milk production or infant weight gain. 357

Pregnancy

. The routine use of macrolide antibiotics prolongs the latency interval and reduces infectious morbidity in women with PPROM, but offers no such prolongation in women with preterm labor and intact membranes, and may even increase the risk of neurodevelopmental compromise. Prolongation of the latency interval is not synonymous with irradication of inflammation. In one study, the administration of both erythromycin and ampicillin rarely eradicated intra-amniotic infection in patients with PPROM. In addition, intra-amniotic inflammation developed in1=3 of women who did not have inflammation on admission despite antibiotic therapy. However, there was a subgroup of women with documented inflammation who demonstrated a decrease in the intensity of the inflammatory process after antibiotic administration. This group likely accounts for the beneficial effects of erythromycin on the latency interval. Erythromycin reduces the frequency of preterm delivery in women with either asymptomatic bacteriuria or symptomatic lower genital tract infections. However, the practice of routine screening for BV in asymptomatic women who are at low risk for preterm delivery cannot be supported based on evidence from the literature. The frequency of GBS resistance renders it a poor selection for prophylaxis. Erythromycin is an effective alternative therapy for the treatment of chlamydial infection. Partner treatment is, overall, cost-effective among women ages 15-29. Though an alternative for the treatment of syphilis in penicillin- allergic patients, placental transport is low (<5%). Thus, erythromycin is not recommended for the treatment of syphilis during pregnancy. Penicillin-allergic women should be desensitized. Recently, a relationship between oral erythromycin and sudden cardiac death was reported in patients also receiving strong inhibitors of CYP3A such as nitroimidazole antifungal agents, diltiazem, verapamil, and troleandomycin; each doubles, at least, the AUC for a CYP3A substrate. The potential implication for obstetrics is real with the growing use of nifedipine as a tocolytic agent in women who may also be treated with antibiotics for preterm PROM. Although not included in the referenced study, nifedipine is also a substrate for CYP3A, suggesting the likelihood for some interaction is high.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Erythromycin crosses the human placenta, achieving an F:M concentration ratio of 0.3.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Erythromycin is excreted into human breast milk, achieving an M:P ratio approximating unity. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. 359

Pregnancy

. Depression is common during and after

Pregnancy

but often goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. Escitalopram is the pure (S-) enantiomer (single isomer) of the racemic citalopram. The published experience with escitalopram during

Pregnancy

consists mostly of inadequately documented case reports. Limited study suggests increased metabolism during the second half of pregnancy. As for most psychotropic drugs, using monotherapy and the lowest effective quantity given in divided doses to minimize the peaks can minimize the risks.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether escitalopram crosses the human placenta. Citalopram does cross the isolated, perfused human placenta with a mean steady-state transfer rate of 9%. The transfer is significantly lower compared with fluoxetine, which suggests lower fetal exposure will occur with citalopram. In contrast, umbilical cord serum measurements reveal that the highest cord:maternal ratios were seen with citalopram and fluoxetine compared to sertraline and paroxetine. Rodent studies are reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. Maternal toxicity, observed at most tested doses, was associated with IUGR. In contrast, the administration of citalopram was associated with CV and skeletal defects.

Breastfeeding

There is no published experience in nursing women. It is unknown whether escitalopram enters human breast milk. Racemic citalopram enters human breast milk, and in one study citalopram and its metabolite M:P ratios were 2:3, but infant citalopram and metabolite plasma concentrations were very low or undetectable. However, there are two reports of infants experiencing somnolence, decreased feeding, and weight loss when breastfed by a citalopram-treated mother. Caution is advised. 361

Pregnancy

. Esmolol is a short-acting b1-blocker employed for the rapid but short-term (9min t/2) control of either hypertension or supraventricular arrhythmia. There are no adequate reports or well-controlled studies of esmolol in pregnant women. The published experience is limited to case reports and small series. It has been used successfully for BP control in women with preeclampsia or pheochromocytoma before induction of general anesthesia, and in women with terbutaline overdose or hypertrophic obstructive cardiomyopathy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Esmolol crosses the human placenta, and fetal bradycardia may continue days after delivery despite the short effect in adults. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Maternal toxicity is associated with embryo lethality.

Breastfeeding

There is no published experience in nursing women. It is unknown whether esmolol is excreted into breast milk.

Pregnancy

. Esomeprazole is the L-isomer of omeprazole. There are no adequate reports or well-controlled studies in pregnant women. Esomeprazole is cost-effective compared with omeprazole in the acute treatment of reflux esophagitis and GERD without esophagitis. These drugs are being used with increasing frequency during pregnancy, and there is a great need for additional study.

Fetal Health

It is unknown whether esomeprazole crosses the human placenta. The F:M ratio of omeprazole at steady state in sheep is about 0.5. The findings of an epidemiologic study including 600 pregnancies is reassuring. In another study run by the European Network of Teratology Information Services, the rates of major anomalies was compared among pregnant women exposed to omeprazole, lanzoprazole, or pantoprazole and a control group. They followed 295 pregnancies exposed to omeprazole (233 in the 1st trimester [T1]), 62 to lansoprazole (55 in T1) and 53 to pantoprazole (47 in T1), along with 868 controls. The rates of major congenital anomalies did not differ between the exposed and control groups and there were no differences when exposure was limited to the 1st trimester after exclusion of genetic, cytogenetic, or infectious anomalies. Rodent studies are likewise reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether esomeprazole is excreted into breast milk. As esomeprazole is the L-isomer of omeprazole, the risks should be similar.

Pregnancy

. There is no published experience with estazolam during pregnancy. Other drugs of this class such as diazepam are considered to be relatively contraindicated during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether estazolam crosses the human placenta. Transplacental movement of similar drugs is known to occur, and neonatal depression is reported. (See Diazepam.)

Breastfeeding

There is no published experience in nursing women. It is unknown whether estazolam enters human breast milk. (See Diazepam.)

Pregnancy

. Estradiol is a naturally occurring estrogen, and as such may have a different risk profile than synthetic or phytoestrogens. It is commonly used for the short-term management of climacteric/postmenopausal symptoms. Conjugated estrogens and estradiol have comparable effects on hot flashes and may have similar short-term adverse effects. Recent studies suggest estrogen plus medroxyprogesterone for the treatment of menopausal symptoms increases the risk of breast cancer and CV disease. There are no indications for estradiol during pregnancy. The effect of estradiol on CV disease remains controversial.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. While diethylstilbestrol and other synthetic/environmental estrogens are recognized teratogens with the potential for transgenerational effects, few studies support this effect for naturally occurring substances like estradiol. There is no clear evidence of fetal harm after inadvertent exposure during the 1st trimester. Some studies have suggested prenatal exposure to estradiol might alter immune programming.

Breastfeeding

Though estradiol is excreted into breast milk and has been reported to reduce the amount of milk produced, it is not effective as an inhibitor of lactation. All pharmacokinetic studies have shown that the transfer to breast milk of both progesterone and estrogen when taking a contraceptive pill is of the same order as natural hormones. Estrogen-containing contraceptives should be initiated after the 6th week of lactation when the lipid profile has returned to normal and the risk of thrombosis is identical to that of the general population.

Pregnancy

. Conjugated estrogens are a mixture of estrogens extracted from natural sources, most commonly pregnant mares? urine. They are widely used for the treatment of hot flashes in climacteric and postmenopausal women. Conjugated estrogens and estradiol have comparable effects on hot flashes and may have similar short-term adverse effects. Unopposed conjugated estrogens have been long known to increase the risk of endometrial cancer. Recent studies demonstrate that estrogen plus 368 medroxyprogesterone for the treatment of menopausal symptoms does not increase the risk of endometrial cancer compared to placebo, but it does increase the risk of breast cancer and CV disease and may increase the risk of ovarian cancer. Although conjugated estrogens plus medroxyprogesterone increases bone density and reduce the risk of fracture in healthy postmenopausal women, there is no net health benefit when the effects of hormone therapy on other important disease outcomes are included in a global model, even in women at high risk of fracture. Many women use conjugated estrogens alone after hysterectomy. The findings of the Women?s Health Initiative Randomized Trial reveal that the use of conjugated estrogens alone increases the risk of stroke by 30%, reduces the risk of hip fracture by 40%, and does not alter the risk of CV disease. There are no indications for conjugated estrogens during pregnancy. (See Estradiol.)

Fetal Health

Estrogen has myriad effects on the developing embryo/fetus; many are poorly understood (see Estradiol).

Breastfeeding

See Estradiol.

Pregnancy

. Esterified estrogens are prepared synthetically from plant sources. There are no indications for esterified estrogens during pregnancy. Recent studies suggest estrogen plus medroxyprogesterone for the treatment of menopausal symptoms increases the risk of breast cancer and CV disease. It has been long known to increase the risk of endometrial cancer. (See Estradiol.)

Fetal Health

Estrogen has myriad effects on the developing embryo/fetus; many are poorly understood (see Estradiol).

Breastfeeding

See Estradiol.

Pregnancy

. Estropipate was formerly known as piperazine estrone sulfate. There are no indications for estropipate during pregnancy. Recent studies suggest estrogen plus medroxyprogesterone for the treatment of menopausal symptoms increases the risk of breast cancer and CV disease. It has been long known to increase the risk of endometrial cancer. (See Estradiol.)

Fetal Health

Estrogen has myriad effects on the developing embryo/fetus; many are poorly understood (see Estradiol).

Breastfeeding

See Estradiol.

Pregnancy

. There are no adequate reports or well-controlled studies of ethacrynic acid in pregnant women. Ethacrynic acid is a potent loop diuretic and rarely indicated. It was used in the past for preeclampsia, pulmonary edema, and diabetes insipidus.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether ethacrynic acid crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Ethacrynic acid is an inhibitor of glutathione transferases, and glutathione is the principle endogenous antioxidant.

Breastfeeding

There is no published experience in nursing women. It is unknown whether ethacrynic acid enters human breast milk. 372

Pregnancy

. There are no adequate reports or well-controlled studies of ethambutol in pregnant women. The published experience consists of relatively small to moderate sized series and case reports. However, untreated tuberculosis poses a significant threat to mother, fetus, and family. Adherence to treatment can be made difficult because of a general fear of any medication and pregnancy-related nausea. What information exists suggests that all 4 first-line drugs for the treatment of tuberculosis (isoniazid, rifampin, ethambutol, and pyrazinamide) have excellent safety records in pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Ethambutol reportedly crosses the human placenta, achieving an F:M ratio approximating unity. There are no reports suggesting an adverse fetal effect. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only small quantities of ethambutol are excreted into breast milk, and it is generally considered compatible with breastfeeding. The dose ingested by the neonate is inadequate to treat tuberculosis.

Pregnancy

. There are no indications for ethinyl estradiol during pregnancy. Recent studies suggest estrogen plus medroxyprogesterone for the treatment of menopausal symptoms increases the risk of breast cancer and CV disease.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. While diethylstilbestrol and other synthetic/ environmental estrogens are recognized teratogens with the potential for transgenerational effects, few studies support this effect for naturally occurring substances like estradiol. There is no clear evidence of fetal harm after inadvertent exposure during the 1st trimester. Some studies have suggested prenatal exposure to estradiol might alter immune programming.

Breastfeeding

Though estradiol is excreted into breast milk and has been reported to reduce the amount of milk produced, it is not effective as an inhibitor of lactation. All pharmacokinetic studies have shown that the transfer to breast milk of both progesterone and estrogen when taking a contraceptive pill is of the same order as natural hormones. Estrogen-containing contraceptives should be initiated after the 6th week of lactation when the lipid profile has returned to normal and the risk of thrombosis is identical to that of the general population.

Pregnancy

. There are no adequate reports or well-controlled studies of ethosuximide in pregnant women. Metabolism does not appear to be significantly altered by pregnancy, only the volume of distribution. Patients may experience drowsiness. Discontinuation of the drug may be considered during

Pregnancy

if the risk of convulsion does not pose a significant health threat to the mother. There is no interaction between ethosuximide and oral contraceptive agents.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Ethosuximide crosses the human placenta, achieving an F:M ratio approximating unity. The associations between ethosuximide and either birth defects or behavioral disorders are unclear.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Ethosuximide is excreted into human breast milk, achieving M:P ratios approximating 0.8-0.9 with an estimated total exposure of 3.6-11mg/kg. Serum concentrations in breastfed neonates range from 15 to 40ng/ml.

Pregnancy

. Ethyl alcohol is one of the most commonly abused drugs during pregnancy. The patient may misrepresent ethyl alcohol use. Antenatal alcohol interviews have the greatest correlation with postnatal outcome and should be part of each prenatal record.

Fetal Health

Ethyl alcohol is the most common teratogen (prevalence 0.5-2/1000 births) and typically reflects chronic consumption. In addition to the well-described fetal alcohol syndrome (pre- and postnatal IUGR, CNS anomalies, and a wide spectrum of malformations, the most typical being the craniofacial features), recent evidence suggests ethyl alcohol may decrease endothelial responses. Tobacco and/or cocaine use are synergistic in their adverse fetal effects. The effects of antenatal exposure on brain development are varied.

Breastfeeding

Ethyl alcohol is excreted into the breast milk, but the quantity ingested by the neonate is too small to have a significant impact.

Pregnancy

. Etidocaine is a rapid-onset (3-5min), long-duration (5-10h) local anesthetic agent with more profound motor block than seen after injection of equianalgesic concentrations of bupivacaine. It is a popular agent in some locales for use in epidural and spinal anesthesia. However, it is not used for labor epidural analgesia due to the motor block. There are no adequate reports or well- controlled studies of etidocaine in pregnant women. Tachycardia may be a sign of intravascular injection.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Etidocaine crosses the human placenta, achieving an F:M ratio approximating 0.3. Uterine blood flow is preserved in the absence of maternal hypotension. Local anesthetics cross when used for epidural, paracervical, pudendal, or caudal nerve blocks and may cause varying degrees of toxicity. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether etidocaine enters human breast milk. Considering the indications and dosing, limited etidocaine use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. There is no published experience with etidronate during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether etidronate crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether etidronate is excreted into human breast milk.

Pregnancy

. Etodolac is an NSAID antipyretic analgesic. There is no published experience during human pregnancy. (See Indomethacin.)

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether etodolac crosses the human placenta. Other NSAIDs do cross. The pharmacologic profile suggests it is likely to have risks similar to those of indomethacin, including oligohydramnios and ductal constriction. Rodent studies performed at doses approximating the MRHD are associated with an increased prevalence of limb abnormalities. Higher doses delayed parturition and increased the perinatal loss rate. (See Indomethacin.)

Breastfeeding

There is no published experience in nursing women. It is not known whether etodolac is excreted into human breast milk. (See Indomethacin.)

Pregnancy

. Etomidate is a short-acting (3-5min) hypnotic drug without analgesic activity. It has little to no effect on cardiac contractility, and is therefore used to induce general anesthesia for cesarean delivery in women with coexisting cardiac disease.

Fetal Health

There are no adequate reports or well-controlled studies of etomidate in human fetuses. Transfer across the rodent placenta occurs, reaching concentrations roughly equal to maternal plasma. Rodent studies reveal no evidence of teratogenicity, though embryo and fetal toxicity occurs, and IUGR is seen when the mothers are exposed long-term to high concentrations.

Breastfeeding

There is no published experience in pregnancy. It is unknown whether etomidate enters breast milk. However, considering the indications and short t/2, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. There are no published studies of etretinate in pregnant women. Drug levels may persist for years after treatment, though the relevance of these levels to subsequent

Pregnancy

outcome is unknown. Case reports note normal outcomes several years after treatment ended. Psoriasis is not lethal, and the use of etretinate is absolutely contraindicated during pregnancy. Women should be tested for

Pregnancy

within 2w of initiating therapy and use effective contraception.

Fetal Health

Etretinate is a human and rodent teratogen, with the majority of fetuses exposed during organogenesis affected. Multiple organ systems are affected, including NTDs, facial dysmorphia, limb and digit malformations, microcephaly, and skeletal defects. Exposed fetuses should be referred to an appropriate fetal evaluation unit. Etretinate has been used to treat harlequin fetuses with improvement in their skin condition but no change in mortality.

Breastfeeding

There is no published experience in nursing women. It is unknown whether etretinate enters human breast milk. It is excreted into rodent milk.

Pregnancy

. There is no published experience with exemestane during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether exemestane crosses the human placenta. It does cross the rodent placenta, achieving concentrations roughly equal to maternal plasma. While increases in embryo resorption and IUGR are seen, there is no increase in the incidence of malformations.

Breastfeeding

There is no published experience in nursing women. It is unknown whether exemestane enters human breast milk. It is excreted into rodent milk.

Pregnancy

. Factor IX is a stabile, lyophilized concentrate either recombinant or made from pooled human plasma. The latter is purified by immunoaffinity chromatography, which reduces the risk of virus transmission. There are no adequate reports or well-controlled studies in pregnant women. The published literature consists of case series and single reports. Factor IX deficiency is typically an X-linked disorder, and thus symptoms occur only in women with unbalanced lyonization. Postpartum hemorrhage is the most common complication, and it occurs more often in women receiving fewer than 4d of factor IX replacement.

Fetal Health

There are no adequate reports or well-controlled studies of factor IX in human fetuses. Placental transfer is unlikely. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether factor IX enters human breast milk. However, any ingested factor would likely be degraded.

Pregnancy

. Famciclovir is metabolized to the active penciclovir. There are no adequate reports or well-controlled studies in pregnant women. With a dosing profile superior to acyclovir, drugs in this class decrease both asymptomatic shedding and the number of clinical recurrences. It is likely that the same is true during pregnancy, a supposition supported by randomized trials and cohort studies demonstrating a lower-than-expected asymptomatic shedding rate. Drug clearance is slower in nonpregnant women compared to men.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether famciclovir crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether famciclovir is excreted in human breast milk. Famciclovir is excreted in concentrations higher than plasma in lactating rats.

Pregnancy

. There are no adequate reports or well-controlled studies of famotidine in pregnant women. There are only rare reports of its use during pregnancy. A single dose of famotidine administered to parturients PO 3h before surgery is more effective neutralizing gastric secretion than omeprazole. One epidemiologic study concluded the use of H2antagonists during

Pregnancy

was associated with a higher prevalence of preterm birth.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Famotidine crosses the placenta, achieving an F:M ratio approximating 0.40. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Famotidine is excreted into human milk to a 386 lesser extent than cimetidine and ranitidine and is thus the preferred agent if a drug of this class is indicated. The daily infant dose has been estimated to be 10.8mcg/kg/d.

Pregnancy

. Epilepsy is a common neurologic disorder affecting 1 million American reproductive-age women. There are no adequate reports or well-controlled studies of felbamate in pregnant women. Drug interactions between enzyme-inducing antiepileptic drugs such as felbamate and hormonal contraceptives are well- documented, increasing the risk of an unplanned pregnancy. Using either a higher-hormone-content oral contraceptive or a second contraceptive is suggested. Planned

Pregnancy

is highly recommended, and counseling before conception crucial, covering folic acid supplementation, optimal control of seizure activity, monotherapy with the lowest effective antiepileptic drug dose, and medication adherence. Drug dose adjustments are often necessary during

Pregnancy

and should be based on clinical symptoms and not solely on serum drug concentrations.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether felbamate crosses the human placenta. It does cross the rodent placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. IUGR was noted.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Felbamate is excreted into human breast milk, though the kinetics remain to be elucidated. Felbamate is excreted into rodent breast milk, and there is a higher death rate in breastfed pups. If Breastfeeding continues, the infant should be monitored for possible adverse effects, the drug given at the lowest effective dose, and

Pregnancy

. There are no adequate reports or well-controlled studies of felodipine in pregnant women. The published experience consists of isolated case reports where felodipine was used successfully for the treatment of severe hypertension during

Pregnancy

without adverse effect. Calcium channel blockers are the most effective tocolytic agents. Felodipine decreases placental blood flow and prolongs parturition in rabbits.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether felodipine crosses the human placenta. Felodipine is associated with an increased prevalence of digital anomalies in rodents possibly secondary to the observed decrease in placental blood flow. Prolonged parturition is associated with an increased perinatal mortality.

Breastfeeding

There is no published experience in nursing women. It is unknown whether felodipine enters human breast milk. It is excreted into rodent milk.

Pregnancy

. There are no adequate reports or well-controlled studies of fenofibrate in pregnant women. One rodent study concludes that pregnant and nonpregnant rats respond differently to fenofibrate, and that high maternal doses were associated with delayed delivery. Since hyperlipidemia is not acutely life-threatening, cessation of medication during

Pregnancy

is suggested.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether fenofibrate crosses the human placenta. Fenofibrate causes IUGR given at doses equivalent to the MRHD, and is embryotoxic and teratogenic (predominantly bony abnormalities) at doses 7-10the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether fenofibrate enters human breast milk.

Pregnancy

. Fenoldopam is an alternative for treatment of a hypertensive crisis if unresponsive to sodium nitroprusside. There are no adequate reports or well-controlled studies of fenoldopam in pregnant women. In isolated systems, it causes relaxation of the rodent myometrium.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether fenoldopam crosses the human placenta. It relaxes thromboxane-constricted human umbilical arteries. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Fenoldopam induces a diuresis in fetal sheep.

Breastfeeding

There is no published experience in nursing women. It is unknown whether fenoldopam enters human breast milk. It is excreted into rodent milk.

Pregnancy

. Fenoprofen is a nonsteroidal, anti-inflammatory, antipyretic agent. There are no adequate reports or well-controlled studies of fenoprofen in pregnant women. Similar to other NSAIDs, it is effective for the relief of episiotomy pain. In rodents, fenoprofen prolongs parturition, and it reduces contractions of isolated myometrium from monkeys and humans.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether fenoprofen crosses the human placenta. Fenoprofen prolongs gestation in rodents, as do other NSAIDs. It is otherwise poorly studied during pregnancy.

Breastfeeding

There is no published experience in nursing women. It is unknown whether fenoprofen enters human breast milk.

Pregnancy

. Fentanyl is a short-acting opiate with considerable risk of abuse. It is often combined during labor with local anesthetics to minimize motor blockade for epidural anesthesia. Fentanyl may be used safely in women with severe preeclampsia. It is a useful adjunct to a paracervical block for suction curettage. The chance 393 of a successful external version is increased by its use with spinal blockade. Its addition to 2.2ml of 0.5% hyperbaric bupivacaine with 0.2ml of morphine 0.2mg intrathecally reduces the incidence and severity of intraoperative and postoperative shivering after spinal anesthesia for cesarean delivery without increasing other Side effects include respiratory depression or arrest, dependency, laryngospasm, bronchospasm, arrhythmias, ileus, cardiac arrest, N/V, weakness, dry mouth, confusion, sweating, euphoria, itching, hypotension, and bradycardia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Fentanyl rapidly crosses the human placenta, achieving an F:M ratio approximating unity. It crosses the fetal blood-brain barrier and has been used for fetal analgesia where a reduction in endorphin levels is demonstrated. Rodent studies are generally reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. It is embryotoxic in rodents. Breastfeeding There are no adequate reports or well-controlled studies in nursing women. Fentanyl enters human breast milk, but is not likely to pose a risk to the neonate of an alert,

Pregnancy

. Iron is absorbed in the duodenum and upper jejunum. About 10% of the delivered dose is absorbed by replete women, and 20-30% in deficient women. Though iron supplementation is widely practiced during

Pregnancy

in the industrialized world, there is no convincing evidence it changes either long- or short- term outcomes. Severe anemia may be an important cause of maternal death, but there is a lack of convincing evidence regarding the risks of mild to moderate maternal anemia. One RCT performed in the US on low-income women with adequate iron stores concluded that the mean birth weight was higher by 108g (p =.03), and the incidence of preterm delivery lower (8% vs 14%; p =.05) with supplementation compared to the control group. In this trial, iron supplementation did not alter the prevalence of SGA infants or 3rd trimester iron status. Women anemic due to iron deficiency should first receive a reticulocytic dose followed by supplementation for the duration of pregnancy. Women with disorders of iron utilization (e.g., thalassemia) should not be routinely supplemented.

Fetal Health

There is no evidence that maternal iron supplementation influences the fetal iron status.

Breastfeeding

Maternal iron supplementation does not alter the iron concentration in breast milk.

Pregnancy

. Fexofenadine is a 3rd-generation antihistamine effective for the symptomatic relief of allergic rhinitis. While increasingly preferred for its nonsedating properties, there are no published controlled trials or population studies of fexofenadine during pregnancy. The published clinical literature consists of a single case report where it was used for the treatment of PUPPP.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether fexofenadine crosses the human placenta. While there is no evidence of teratogenicity in rodents, there is a dose-dependent increase in IUGR and decrease in the survival of pups.

Breastfeeding

There is no published experience in nursing women. It is unknown whether fexofenadine enters human breast milk. However, there is one study of terfenadine, of which fexofenadine is a metabolite. The average M:P ratio was 0.2. The authors estimated the theoretic infant dose was 6.2mcg/kg/d, or <0.5% of the weight adjusted maternal dose. 396

Pregnancy

. There are no adequate reports or well-controlled studies of filgrastim in pregnant women. It has been used to treat severe chronic neutropenia and chemotherapy-induced neutropenia during

Pregnancy

without obvious adverse effect. The published literature is confined to case reports and usually complicated by polypharmacy. 397

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether filgrastim crosses the human placenta. There is no evidence to suggest it is a human teratogen. However, rodent studies using high doses reveal evidence of embryotoxicity, IUGR, and delayed external differentiation.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether filgrastim enters human breast milk.

Pregnancy

. There is no published experience with flavoxate during pregnancy. In nonpregnant women, flavoxate first increases, then decreases, uterine contractions.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether flavoxate crosses the placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. 398

Breastfeeding

There is no published experience in nursing women. It is unknown whether flavoxate enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of flecainide in pregnant women. Flecainide has been used successfully for the treatment of maternal arrhythmias during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Flecainide rapidly crosses the placenta, achieving an F:M ratio approximating unity in the early 3rd trimester, and like digoxin, is concentrated in AF. However, better controlled studies in the baboon suggest an F:M ratio of 0.49. An accepted second-line agent for the treatment of fetal SVT, the popularity of flecainide as a first-line agent, especially with hydrops, is growing. An elevated umbilical venous pressure, such as that associated with hydrops fetalis, reduces the placental transport of both flecainide and digoxin.

Breastfeeding

Though flecainide is excreted in human breast milk, achieving an M:P ratio approximating 2.5, the quantity consumed would be 399 unlikely to produce a neonatal plasma level above 100ng/ml, a subtherapeutic level.

Pregnancy

. There are no adequate reports or well-controlled studies of fluconazole in pregnant women. It has been used for the treatment of coccidioidomycosis during

Pregnancy

and Candida sepsis postpartum. The systemic antifungal drug with which there has been the most experience is amphotericin B.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether fluconazole crosses the human placenta. Four children are described with a similar and rare pattern of anomalies. The features include brachycephaly, abnormal facies, abnormal calvarial development, cleft palate, femoral bowing, thin ribs and long bones, arthrogryposis and congenital heart disease. Each was associated with chronic, parenteral use in the 1st trimester. Limited duration oral therapy is unlikely to pose a teratogenic risk. Fluconazole does not appear to increase the risks of IUGR or preterm delivery. It has been used for the treatment of congenital candidiasis. Rodent studies conducted at multiples of the MRHD revealed a variety of ossification defects considered consistent with inhibition of estrogen synthesis. There was an increased risk of cleft palate in rats when combined with phenytoin. Similar concerns have been reported in humans.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Fluconazole enters human breast milk at concentrations similar to maternal plasma. It is generally recommended that Breastfeeding be avoided. 401

Pregnancy

. There are no adequate reports or well-controlled studies of flucytosine in pregnant women. It has been used during

Pregnancy

for the treatment of cryptococcal meningitis and pneumonia, and Candida septicemia. The systemic antifungal drug with which there has been the most experience is amphotericin B.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether flucytosine crosses the human placenta. While rat studies revealed teratogenicity at doses analogous to human doses, no adverse effects were found in mice, rabbits, and primates.

Breastfeeding

There is no published experience in nursing women. It is unknown whether flucytosine enters human breast milk.

Pregnancy

. Fludrocortisone is a synthetic adrenal steroid possessing potent mineralocorticoid and glucocorticoid activities. There are no adequate reports or well-controlled studies of fludrocortisone in pregnant women. The published literature consists of cases reports and small series. It has been used without complication for the treatment of adrenal insufficiency during pregnancy. The needed replacement dose often increases and should be guided by serial biochemical measurements. Women treated for salt-losing, congenital adrenal hyperplasia conceive and complete pregnancies successfully.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Though many corticosteroids in rats have been associated with such anomalies as cleft palate, there is controversy whether corticosteroids are as a class weak teratogens in humans.

Breastfeeding

There is no published experience in nursing women. It is unknown whether fludrocortisone enters human breast milk, though other corticosteroids are excreted at low concentrations into human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of flumazenil in pregnant women. The published literature is limited to case reports where it was used successfully for the treatment of benzodiazepine overdose during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Since flumazenil can apparently reverse maternally administered diazepam in the both the fetus and neonate, it likely crosses the human placenta. Rodent studies reveal no evidence of teratogenicity, but embryotoxicity occurs at high doses. Behavioral changes were noted in rat pups after late

Pregnancy

exposure.

Breastfeeding

There is no published experience in nursing women. It is unknown whether flumazenil enters human breast milk. Considering the indication, limited or one-time flumazenil use is unlikely to pose a clinically significant risk to the Breastfeeding neonate. 405

Pregnancy

. There is no published experience with flunisolide during pregnancy, though inhaled corticosteroids are a cornerstone of asthma therapy. They are used widely during

Pregnancy

without apparent adverse effects.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether flunisolide crosses the human placenta. In rodents, flunisolide is both embryotoxic and teratogenic at 100the MRHD. Although systemically administered corticosteroids are teratogenic in some rodents, and a weak effect in humans cannot be excluded, the concentration of drug absorbed systemically suggests the risk of a significant fetal effect is low. This conclusion is supported by a recent meta- analysis of inhaled steroid usage during pregnancy. 406

Breastfeeding

There is no published experience in nursing women. It is unknown whether flunisolide enters human breast milk. Considering the concentration and quantity absorbed systemically, it is unlikely the plasma level achieved will be clinically relevant to lactation.

Pregnancy

. There is no published experience with fluocinolone during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether fluocinolone crosses the human placenta. While systemically administered corticosteroids, including fluocinolone, are teratogenic in some rodents, and a weak effect in humans cannot be excluded, the concentration of drug absorbed systemically suggests the risk of an adverse fetal effect is low.

Breastfeeding

There are no reports in nursing women. It is unknown whether fluocinolone enters human breast milk. However, considering the concentration and quantity absorbed systemically, it is unlikely the plasma level achieved will be clinically relevant to lactation.

Pregnancy

. There are no adequate reports or well-controlled studies of fluorouracil in pregnant women. Fluorouracil is most commonly used during

Pregnancy

in the 2nd and 3rd trimesters for the treatment of metastatic breast cancer, where it is often combined with doxorubicin and cyclophosphamide (FAC). While it should be used only when there is significant risk for the mother?s survival, breast cancer can be treated with FAC chemotherapy during the 2nd and 3rd trimesters without significant short-term complications for the majority of children exposed to chemotherapy in utero.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Fluorouracil apparently crosses the human placenta, since maternal administration is associated with fetal immunosuppression. The few published epidemiologic studies support multiple case reports of normal

Pregnancy

outcome after early exposure. Little is known about the long-term effects of intrauterine exposure to fluorouracil. Fluorouracil crosses the rodent placenta and produces a variety of defects involving the skeleton and palate. It is embryotoxic to the rodent. The malformations associated with in utero exposure to FAC are highly variable, but growth deficiency and anomalies of the 408 craniofacial region and limbs are most common. The pattern appears to be directly related to the age at and duration of exposure, rather than to the specific drug itself.

Breastfeeding

There is no published experience in nursing women. It is unknown whether fluorouracil enters human breast milk.

Pregnancy

. Depression is common during and after pregnancy, but typically goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. A fluoxetine dose of 20-40mg/d 409 results in relatively low trough fluoxetine-norfluoxetine concentrations during

Pregnancy

(range, 317-850nmol/L) and the mean norfluoxetine/fluoxetine metabolic ratio is 2.4higher during late

Pregnancy

compared to 2mo postpartum. This suggests increased clearance, which can be explained at least in part by increased demethylation of fluoxetine by CYP2D6 and is consistent with the observation that many pregnant women require an increase in their dose to maintain clinical efficacy. Fluoxetine is effective treatment for postpartum depression, and is as effective as a course of cognitive-behavioral counseling in the short term.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Fluoxetine crosses the human placenta, achieving F:M ratios approximating 0.9. This is significantly higher than the ratios achieved with either sertraline or paroxetine and similar to citalopram. Maternal doses predict the umbilical cord concentration. Prospectively ascertained

Pregnancy

outcomes after SSRIs, mainly fluoxetine, conflict on the potential for a modest teratogenic effect. There are differences in birth weight and acute neonatal outcome between treated and untreated pregnancies. In one study of 20 pregnancies, there was a 4-fold difference in the serotonergic symptom score of newborns during the first 4d of life between treated and control groups. The exposed infants had significantly lower cord blood 5-hydroxyindoleacetic acid (5- HIAA) levels. There was an inverse correlation between the serotonergic symptom score and the umbilical vein 5-HIAA concentrations in the exposed infants. The long-term implications of these findings are unclear. Exposure throughout gestation does not adversely affect cognition, language development, or the temperament of preschool and early school-age children. In sheep, fluoxetine has transient effects on fetal behavioral and acid-base status. Rodent studies too are reassuring from the standpoint of structural birth defects, though the rates of IUGR and stillbirth are higher in rats treated with multiples of the MRHD. Prolonged prenatal SSRI exposure in rats is associated with reduced behavioral pain responses and increased parasympathetic cardiac modulation in recovery following an acute neonatal noxious event. However, a recent rodent study found that maternal exposure to fluoxetine has transient effects on fetal behavioral and acid-base status during

Pregnancy

and lactation that result in enduring behavioral alterations in the pups throughout life. Others conclude that the behavioral affects are not permanent.

Breastfeeding

Maternal serum and peak breast milk concentrations of fluoxetine and its active metabolite, norfluoxetine, predict nursing infant serum norfluoxetine concentrations. The mean estimated infant exposure from the breast milk of women taking 20-40mg/d to fluoxetine-norfluoxetine is 2.4% and 3.8% of the maternal weight-adjusted daily dose at 2w and 2mo of age, respectively. Neonatal serum concentrations are typically low in women taking 20mg/d or less. Thus, Breastfeeding is not contraindicated.

Pregnancy

. There is no published experience with fluoxymesterone during pregnancy. There are no recognized indications for its use during pregnancy.

Fetal Health

There are no studies in human fetuses. It is unknown whether fluoxymesterone specifically or an active metabolite crosses the human placenta. Androgens are recognized human teratogens leading to masculinization of the female fetus. 412

Breastfeeding

Fluoxymesterone is ineffective for the suppression of lactation and is no longer used. It is unknown whether fluoxymesterone enters human breast milk.

Pregnancy

. Fluphenazine is a long-acting parenteral antipsychotic typically used in institutional settings. There are no adequate reports or well-controlled studies in pregnant women. Consistent with its biochemistry, fluphenazine increases maternal prolactin.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether fluphenazine crosses the human placenta. Rodent studies reveal bone and CNS malformations. The incidence of these malformations increases significantly when diphenylhydantoin is administered concurrently. Peroxidative bioactivation of phenothiazines to their 413 cation radical by human placental peroxidase may be one mechanism of developmental toxicity.

Breastfeeding

There is no published experience in nursing women. It is unknown whether fluphenazine enters human breast milk.

Pregnancy

. There are reports of flurandrenolide use during pregnancy.

Fetal Health

There are no reports or well-controlled studies of flurandrenolide in human fetuses. Rodent teratogenicity studies have apparently not been performed. While systemically administered corticosteroids are teratogenic in some rodents, and a weak effect in humans cannot be excluded, the concentration of drug absorbed systemically if applied to a small area suggests the risk of a significant fetal effect is low. 414

Breastfeeding

There is no published experience in nursing women. It is unknown whether flurandrenolide enters human breast milk. It is unlikely the limited systemic concentration achieved after application to a small area is clinically relevant to lactation.

Pregnancy

. There are no adequate reports or well-controlled studies of flurazepam in pregnant women. There are other hypnotics on the market with better pharmacologic and safety profiles, such as zolpidem. Prolonged use of hypnotics is not advised.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Flurazepam crosses the human placenta, though the kinetics remain to be elucidated. Benzodiazepines such as diazepam and chlordiazepoxide may be associated with an increased risk of malformations after 1st trimester exposure. Rodent teratogenicity studies with flurazepam specifically have not apparently been performed. Neonatal depression was reported in a neonate of a woman taking flurazepam for the 10d preceding delivery. The long-term neurologic effects of in utero exposure are unknown.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Older abstracts suggest flurazepam enters human breast milk. 415

Pregnancy

. Flurbiprofen is a nonselective COX inhibitor with analgesic, antipyretic, and anti-inflammatory activities. There are no adequate reports or well-controlled studies of flurbiprofen in pregnant women. It is equivalent to aspirin and superior to codeine as an analgesic for postpartum uterine pain. It is unknown whether flurbiprofen offers any advantage over other, similar NSAIDs. Flurbiprofen prolongs rat parturition, as do most NSAIDs.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Flurbiprofen crosses the human placenta. Other NSAIDs cause ductus arteriosus constriction and oligohydramnios secondary to fetal oliguria. Flurbiprofen is known to do so in rats. Rodent studies are generally reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than that used clinically. High doses in the rodent are associated with embryotoxicity and increased perinatal mortality secondary to delayed parturition.

Breastfeeding

The elimination half-life of flurbiprofen during early lactation is slightly prolonged (mean 4.8h) compared to adult males. The peak plasma concentrations are comparable to those reported for healthy volunteers. In 10 of 12 women (3-5d postpartum), the flurbiprofen concentration in breast milk was less than 0.050mcg/ ml. The remaining women did not exceed 0.07mcg/ml. This concentration is insufficient to pose a risk to the Breastfeeding neonate.

Pregnancy

. There are no adequate reports or well-controlled studies of fluticasone in pregnant women. Fluticasone is a popular agent in women with asthma and commonly encountered during pregnancy. Case series are reassuring. It is not effective for the treatment of

Pregnancy

rhinitis. Once-daily budesonide nasal spray, fluticasone nasal spray, mometasone furoate nasal spray, and triamcinolone aqueous nasal spray have similar efficacy and safety profiles for treatment of allergic rhinitis in adults. Differences in sensory attributes, experience during pregnancy, and cost may contribute to better patient acceptance of one versus another. A recent meta-analysis concluded that inhaled or nasal corticosteroids do not increase the rates of adverse obstetric outcomes.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether fluticasone crosses the human placenta. However, inhaled or nasal corticosteroids alone do not adversely affect fetal growth or placental function. While systemically administered corticosteroids, including fluticasone, are teratogenic in some rodents and a weak effect in humans cannot be excluded, the concentration of drug absorbed suggests the risk of an adverse fetal effect is low. There are no documented epidemiologic studies with IN corticosteroids during pregnancy; however, inhaled corticosteroids have not been incriminated as teratogens and are commonly used by pregnant 418 women who have asthma. Less than 0.1% of an inhaled dose crosses the rodent placenta.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether fluticasone enters human breast milk. Measurable but small amounts enter rat breast milk. However, considering the concentration and quantity absorbed systemically, it is unlikely the plasma level achieved will be clinically relevant to lactation.

Pregnancy

. Fluvastatin is a competitive inhibitor of the enzyme responsible for the conversion of HMG-CoA to mevalonate, a precursor of cholesterol. There are no adequate reports or well-controlled studies of fluvastatin in pregnant women. Hyperlipidemia is a chronic illness, and discontinuing treatment during

Pregnancy

is unlikely to compromise patient care. Published experience is confined to a case report. However, there is an unexpected high maternal mortality rate in rats during lactation. Supplementation with mevalonic acid completely blocks and/or ameliorates death, cardiac myopathy, and other adverse effects. Thus, the adverse maternal effects result from exaggerated pharmacologic activity at the dose levels administered (i.e., inhibition of the enzyme HMG-CoA reductase, its immediate product mevalonic acid, and cholesterol biosynthesis). It is not known whether

Pregnancy

enhances the toxicity of fluvastatin in humans.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is not known whether fluvastatin crosses the placenta. While lovastatin, simvastatin, and atorvastatin are inhibitors for P-glycoprotein and may be substrates for this transporter, fluvastatin and pravastatin consistently demonstrate no significant inhibition of P-glycoprotein. In rodents, fluvastatin is associated with delayed and abnormal skeletal development. There is one report of VATER in the child of a woman who took fluvastatin during the 1st trimester. Similar-class drugs are associated with rare reports of malformations.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Fluvastatin apparently enters human breast milk, as the manufacturer reports an M:P ratio of 2.0. The affect on the Breastfeeding neonate is unknown.

Pregnancy

. There are no adequate reports or well-controlled studies of fluvoxamine in pregnant women. It is chemically unrelated to the other SSRIs. The few published case reports suggest no adverse effects when used at recommended doses.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Though the kinetics need further clarification, about one third of the maternal fluvoxamine dose crosses the human placenta and is excreted into the AF. This is about half of the placental transfer of fluoxetine. There is no evidence of teratogenicity or any other adverse effect in humans after 1st trimester exposure. A recent meta-analysis concluded that SSRIs do not increase the risk of major, CV, and minor 421 malformations but do increase the risk of spontaneous abortion. However, newborns exposed to SSRI antidepressants toward the end of

Pregnancy

can show signs of agitation, altered muscle tone, and breathing. These neonatal symptoms have been noted with citalopram, fluoxetine, fluvoxamine, paroxetine, and sertraline. An estimated 20-30% of newborns exposed to an SSRI toward the end of

Pregnancy

are affected. The symptoms are variously attributed to withdrawal or to the drug itself. There is no consensus on the treatment of affected newborns, but close monitoring is mandatory. SSRI antidepressants are not teratogenic in animals. Prolonged prenatal SSRI exposure in rats is associated with reduced behavioral pain responses and increased parasympathetic cardiac modulation in recovery following an acute neonatal noxious event. However, a recent rodent study found that maternal exposure to fluoxetine has transient effects on fetal behavioral and acid-base status during

Pregnancy

and lactation that resulted in enduring behavioral alterations in the pups throughout life. At higher doses, many pups died from a dilated cardiomyopathy. Others conclude that the behavioral affects are not permanent.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Fluvoxamine is excreted in low concentrations into human breast milk, but the resulting neonatal levels are below the limit of detection.

Pregnancy

. Suboptimal preconception folate and vitamin B6reserves, especially when combined, may increase the risk of spontaneous abortion. Women who become pregnant before folate restoration is complete have an increased risk of folate insufficiency at conception and during pregnancy. As a consequence, they may be at increased risk of preterm birth. Recent epidemiologic investigation suggests a reduction in the rates of preterm birth and low birth weight since the introduction of widespread food fortification. Women with HIV also show improved

Pregnancy

outcomes when supplemented with folate.

Fetal Health

NTDs and other

Pregnancy

complications are linked to impaired MTHFR function. Each doubling of the serum folate concentration roughly halves the risk of an NTD. It is suggested that high levels of folate supplementation might blunt the negative impact of antiepileptic drugs. More recently, evidence has emerged that vitamin B12deficiency also increases the risk of a child with an NTD. Placental folate transfer is not compromised in IUGR pregnancies. Knockout of folate receptors in mice, and knock-down of folate receptors by antisense oligonucleotides at day 8, or antibodies to folate receptor, results in profound developmental abnormalities ranging from NTDs to neurocristopathies such as cleft lip and cleft palate, cardiac septal defects, and eye defects. These abnormalities can be prevented by supplying folate into cells via alternative pathways. The high prevalence of mutated MTHFR genotypes in spontaneously aborted embryos supports the potentially protective role of periconceptional folic acid supplementation.

Breastfeeding

Maternal folate stores are depleted during lactation without supplementation. Supplementation minimizes maternal loss and significantly increases the concentration of folate in milk.

Pregnancy

. There are no adequate reports or well-controlled studies of fomepizole in pregnant women. The published experience consists of several case reports. However, the risks of ethylene or methanol toxicity to mother and fetus outweigh any theoretic risk of the drug.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether fomepizole crosses the placenta. However, both methanol and ethylene glycol do cross the human placenta. Animal reproduction studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether fomepizole enters human 425 breast milk. However, it is unlikely a patient requiring treatment will breastfeed during that period.

Pregnancy

. Fondaparinux is the first in a new class of heparinoid antithrombotic agents developed for the prevention and treatment of VTE. It inhibits thrombin generation by selectively inhibiting factor Xa. Fondaparinux is rapidly absorbed, reaching its maximum concentration in approximately 2h. The terminal t/2 of 13-21h permits once-daily dosing. Fondaparinux?s reproducible linear pharmacokinetic profile suggests individual dose adjustments will not be required for the vast majority of the nonpregnant population and that there will be no need for 426 routine hemostatic monitoring. At therapeutic concentrations (>2mg/L), fondaparinux exhibits >94% binding to its target protein, antithrombin. The current experience in pregnancy, though encouraging, is confined to a series of case reports. It is unknown whether

Pregnancy

alters clearance of fondaparinux. Though conceptually superior, there is inadequate clinical study to favor its use over LMWH or unfractionated heparin.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. In vitro, fondaparinux does not cross the human placenta, suggesting the fetus is not directly at risk.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether fondaparinux enters human breast milk.

Pregnancy

. Formoterol is a long-acting b-mimetic agent used for asthma prophylaxis. It is not for acute treatment. There are no adequate reports or well-controlled studies of formoterol in pregnant women. Only 33 pregnant women were reported to have used formoterol in a post-marketing survey. No adverse effects were noted. There is some reduction in rodent myometrial contractility when studied in vitro. In one rodent study of lipopolysaccharide (LPS)-triggered preterm labor, formoterol reduced the cytokine response to LPS.

Fetal Health

There are no adequate reports or well-controlled studies of formoterol in human fetuses. Rodent studies are reassuring, revealing delayed ossification, IUGR, and increased perinatal mortality only at doses >2000the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether formoterol enters human breast milk. The transfer of similar agents, such as terbutaline, is very low.

Pregnancy

. Foscarnet exerts its antiviral activity by a selective inhibition at the pyrophosphate binding site on virus-specific DNA polymerases. There are no adequate reports or well-controlled studies of foscarnet in pregnant women, and the indications are limited. Foscarnet was used successfully during

Pregnancy

in 1 woman with AIDS for the treatment of genital acyclovir-resistant HSV type 2, and in another HIV-infected woman with myeloradiculitis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether foscarnet crosses the human placenta. Rodent studies were for the most part reassuring, revealing a modest increase in minor skeletal abnormalities.

Breastfeeding

There is no published experience in nursing women. It is unknown whether foscarnet enters human breast milk. However, it is concentrated in rat breast milk.

Pregnancy

. Fosfomycin is an orally active, broad-spectrum bactericidal agent that has the advantage of single-dose administration. In several controlled trials conducted in pregnant women, it was similar in efficacy to other commonly used agents.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Fosfomycin crosses the human placenta, though the kinetics remain to be clarified. It does not reach an F:M ratio of unity. Rodent studies are reassuring; fetal toxicity is seen only when the dose used produced maternal toxicity.

Breastfeeding

There is no published experience in nursing women. It is unknown whether fosfomycin enters human breast milk.

Pregnancy

. There is no published experience with fosinopril, a long-acting ACEI, during pregnancy. Fosinopril is rarely if ever necessary during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether fosinopril crosses the human placenta. However, this class of drugs is known to have adverse human fetal renal effects leading to disability or death and should be considered contraindicated during pregnancy. Similar effects occur with fosinopril in rodents.

Breastfeeding

There is no published experience in nursing women. The manufacturer reports low levels of fosinopril in human breast milk.

Pregnancy

. Fosphenytoin is converted in vivo to phenytoin. There are no adequate reports or well-controlled studies of fosphenytoin in pregnant women, but the risks should be similar to phenytoin. The risk of seizure during

Pregnancy

may rise because of increased clearance. Maternal serum levels should be monitored throughout gestation.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Its risk profile should be similar to phenytoin.

Breastfeeding

There is no published experience in nursing women. It is unknown whether fosphenytoin enters human breast milk. Its profile should be similar to phenytoin.

Pregnancy

. There is no published experience with frovatriptan during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies of frovatriptan in human fetuses.

Breastfeeding

There is no published experience in nursing women. It is unknown whether frovatriptan enters human breast milk. Considering the limited dosing regimen and the safety of similar- class agents, frovatriptan is likely compatible with breastfeeding. If desired, the patient may pump her breasts for 24h and then resume breastfeeding.

Pregnancy

. Furazolidone is a metabolite of nitrofurantoin and should have a similar degree of safety during pregnancy. It is an alternative treatment for giardiasis. There are no adequate reports or well-controlled studies in pregnant women. (See nitrofurantoin.)

Fetal Health

There are no adequate reports or well-controlled studies of furazolidone in human fetuses (see nitrofurantoin).

Breastfeeding

There is no published experience in nursing women. Furazolidone is excreted into rodent breast milk. (See nitrofurantoin.)

Pregnancy

. There are no adequate reports or well-controlled studies of furosemide in pregnant women. It is one of the drugs of choice for the treatment of CHF and/or pulmonary edema during pregnancy. High concentrations of furosemide dilate the capacitance vessels and assist the reduction in preload. The long clinical experience for the noted indications is reassuring. In one study of women with preeclampsia, furosemide caused a significant decrease in the intervillous blood flow. This likely reflects an already contracted intravascular volume. In another study of women with hyperdynamic cardiac outputs (COs), furosemide initiated at 22w gestation decreased CO and stroke volume (1.2?0.2L/min and 17?3ml, respectively), whereas total pulmonary resistance increased (101?26 dyne.sec.cm?5; p <.001 for all) after 2.9?1.4w. However, the hemodynamic improvement did not approach that expected for pregnancy. Thus, while furosemide improved the hyperdynamic circulation, it neither lowered BP nor caused clinically significant vasoconstriction. In rabbit studies, a high dose of furosemide was associated with unexplained maternal deaths.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Furosemide crosses the human placenta, achieving an F:M ratio approximating unity after 8-10h. It is unclear, however, how responsive the fetal kidney is to it, and the impact of gestational age on that response. Direct administration of furosemide for fetal therapy, typically in association with hydrops, has been frequently reported. However, no corresponding diuresis has been documented. In rodents, an effect on newborn urine concentrating ability is reported after in utero exposure. An increased prevalence was also noted in one mouse study. Though fetal sheep absorb it from AF presumably via a transmembrane mechanism, direct administration fails to generate a fetal diuresis. In addition, there is no fetal diuresis after administration to the gravid ewe. In summary, the impact of furosemide on the fetus is unclear and likely small.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Furosemide does enter human breast milk, but the kinetics remain to be elucidated. It is unlikely one-time or limited use would cause harm during lactation.

Pregnancy

. Gabapentin is a 2nd-generation anticonvulsant used mainly as an adjunct. While there is little published experience during

Pregnancy

and lactation, the limited study available suggests a higher safety margin relative to 1st-generation agents. The impact of

Pregnancy

upon gabapentin metabolism apparently has not been studied. The dose may require adjustment during pregnancy, and should be based on both serum concentration and clinical symptoms. Gabapentin has been used for chronic headache during early pregnancy. While a relationship between hormones and seizure activity exists in many women, good options for catamenial epilepsy remain elusive. And while interactions between enzyme-inducing anticonvulsants and contraceptives are well documented, this is not true for gabapentin. Patients should be counseled to plan pregnancy, and informed of the value of folate supplementation, the importance of medication adherence, and the risk of teratogenicity. Gabapentin has been given for Restless Leg Syndrome, a disorder reportedly increased during pregnancy, and appears to reduce both the frequency and the severity of hot flashes in postmenopausal women in a dose-dependent manner.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Gabapentin crosses the human placenta, achieving a F:M ratio of 1.7 (range 1.3-2.1). Limited observations suggest active transport of gabapentin, with accumulation in the fetus. This suggests the presence of L-type amino acid transporter 1 in the placenta. There was no evidence of human teratogenicity in a small post-marketing study. Rodent studies reveal fetotoxicity and an increased prevalence of minor malformations, including skeletal abnormalities (skull, spine, and limbs) and hydronephrosis.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Gabapentin is excreted into human breast milk. 438 In one series, the M:P ratio was 1.0 (range, 0.7-1.3) from 2w to 3mo. The infant dose was estimated at 0.2-1.3mg/kg/day, equivalent to 1.3-3.8% of the weight-normalized dose received by the mother. Thus, the drug is absorbed by the neonate. The plasma concentration in the breastfed infants was approximately 12% of the mother?s plasma level, but no adverse effects were observed. Absent a larger experience, the infant should be monitored for possible adverse effects, the drug given at the lowest effective dose, and Breastfeeding avoided at times of peak drug levels.

Pregnancy

. There is no published experience with gadoversetamide during pregnancy. 439

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether gadoversetamide crosses the human placenta. It does cross the rodent placenta. Limited rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR.

Breastfeeding

There is no published experience in nursing women. It is unknown whether gadoversetamide enters human breast milk. It is excreted in rat breast milk. Breastfeeding women should consider discarding their milk after injection for the first 72h after the MRI.

Pregnancy

. There is no published experience in pregnancy. In light of the natural history of Alzheimer?s disease, galantamine is unlikely to be required during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether galantamine crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses 440 higher than those used clinically. Galantamine has the therapeutic potential to protect the brain from glutamate toxicity.

Breastfeeding

There is no published experience in nursing women. It is unknown whether galantamine enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Case reports include ganciclovir use during the 1st trimester in 1 woman with a liver transplant and another with a kidney transplant, and in a third with CMV hepatitis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Ganciclovir crosses the human placenta by passive diffusion. It has been administered directly to CMV-infected fetuses with sonographically detected sequelae 441 and no clear success: the viral load declined but the fetus died. It also has been used to treat an infected fetus who developed primary CMV after maternal primary infection associated with a renal transplant. In this instance, the fetal CMV was reportedly erradicated. Postnatally, ganciclovir remains the drug of choice for the treatment of symptomatic neonatal CMV; it is not curative, but rather ameliorates sequelae. Ganciclovir is embryotoxic in rats and mice. In rabbits, it is associated with cleft palate, micropthalmia, renal agenesis, and hydrocephaly.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Fetuses with brain or abdominal findings have the worst prognoses and are potential candidates for fetal therapy. It is unknown whether ganciclovir enters human breast milk. Ganciclovir enters rat breast milk by passive diffusion, reaching near-maternal serum levels. However, it is usually considered compatible with Breastfeeding considering its neonatal application.

Pregnancy

. Gatifloxacin is a well-absorbed oral quinolone. There is no published experience with gatifloxacin during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether gatifloxacin crosses the human placenta. Rodent studies using multiples of the MRHD reveal an increased risk of skeletal abnormalities and neonatal death rate.

Breastfeeding

There is no published experience in nursing women. It is unknown whether gatifloxacin enters human breast milk. Gatifloxacin does enter rat milk, and caution is recommended during lactation.

Pregnancy

. There are no adequate reports or well-controlled studies of gemfibrozil in pregnant women. Hyperlipidemia is a chronic illness. Discontinuation of therapy during

Pregnancy

is in most instances unlikely to alter the long-term outcome. Case reports document uncomplicated use of gemfibrozil in pregnant women with either hypertriglyceridemia or familial chylomicronemia or complications there of.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Based on a single case report, gemfibrozil crosses the human placenta. The level of gemfibrozil in the fetal venous and arterial cord blood was within the expected therapeutic range for adults. Despite extremely low fat in the maternal diet, the levels of essential fatty acids measured in the mother and in the 444 fetal blood immediately postpartum were normal. Rodent studies reveal a dose-related increase in skeletal abnormalities at twice the MRHD.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether gemfibrozil enters human breast milk. The offspring of treated rodents have reduced weight during neonatal and weaning periods.

Pregnancy

. Gentamicin is commonly used in obstetric patients for the treatment of infections such as pyelonephritis. Though its clearance is increased during

Pregnancy

and in the puerperium, routine monitoring of peak and trough levels is not required in otherwise healthy women with normal renal function. Coupled with clindamycin, it remains standard for the treatment of puerperal endomyometritis. Once-daily treatment postpartum (5mg/kg) with clindamycin is as effective as and cheaper than tid dosing. Once the endometritis has resolved on IV therapy, there is no need for further oral therapy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Gentamicin crosses the human placenta, reaching an F:M ratio approximating unity. In rodents, placental transfer is greater early than late gestation. Gentamicin interferes with renal protein reabsorption in fetal rats, and depresses body weights, kidney weights, and median glomerular counts in newborn rats when administered systemically at multiples of the MRHD. However, the evidence for human fetal gentamicin toxicity is weak. In utero exposure to gentamicin does not appear to cause increase the risk of audiologic impairment. There is no evidence to support the practice in some locales of using gentamicin for ophthalmia neonatorum prophylaxis.

Breastfeeding

Gentamicin enters human breast milk. In one study, the mean M:P gentamicin ratios were 0.11 and 0.44 at 1 and 7h, respectively., However, only trace amounts are absorbed by the Breastfeeding child.

Pregnancy

. There is no published experience with glatiramer during pregnancy. As a result, most experts recommend discontinuing glatiramer prior to conception.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether glatiramer crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether glatiramer enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of glimepiride in pregnant women. The published experience is limited to case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether glimepiride crosses the human placenta. There is evidence suggesting other 2nd- generation sulfonylureas cross poorly. However, there is a case report of a newborn with persistent hyperinsulinemic hypoglycemia after long-term in utero exposure to glimepiride. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Fetal losses occurred at doses approximating 4000the MRHD.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether glimepiride enters human breast milk.

Pregnancy

. There is no published experience with glipizide during pregnancy. Some oral hypoglycemic agents are potentially attractive for the treatment of gestational or type 2 diabetes mellitus during pregnancy. However, their use at the present time should probably be confined to formal protocols.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. About 6% of the maternal dose of glipizide crosses the isolated human placenta. Only glyburide transport is lower. No teratogenic effects were found in rodents, though fetal loss occurs across a range of doses.

Breastfeeding

There is no published experience in nursing women. It is unknown whether glipizide enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. There is, however, a long, reassuring clinical experience of glucagon use during pregnancy, typically in diabetic women with insulin-induced severe hypoglycemia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Glucagon does not appear to cross the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience with glucagon in nursing women. It is unknown whether it is excreted in human breast milk. However, glucagon is not active when ingested, as it is destroyed in the GI tract before absorption.

Pregnancy

. A growing body of investigation indicates that glyburide is an effective alternative to insulin in women with either gestational or Type II diabetes, where it is more cost-effective than insulin.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Less than 2% of the maternal glyburide dose crosses the isolated perfused human placenta, findings confirmed in vivo. Back transport by BCRP appears to be the principle mechanism limiting glyburide efflux across the placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether glyburide enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of glycerin in pregnant women. Maternal risks are related to abuse of the product.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. However, maternal systemic absorption of glycerin is low.

Breastfeeding

There is no published experience in nursing women. However, maternal systemic absorption of glycerin is low, suggesting the risk to the Breastfeeding neonate is minimal.

Pregnancy

. Glycopyrrolate reduces nausea after spinal anesthesia in pregnant women. It also reduces the prevalence of hypotension after epidural anesthesia in women with normal HRs to a similar degree as ephedrine. It may increase the risk of significant tachycardia when given with a b-mimetic agent.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether glycopyrrolate crosses the human placenta. Transfer is limited in the ewe, achieving a peak F:M ratio of 0.13. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether glycopyrrolate enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of gold sodium thiomalate in pregnant women. It is important to perform a urinalysis before each injection because of the risk of maternal renal toxicity.

Fetal Health

There are no adequate reports or well-controlled studies of gold sodium thiomalate in human fetuses. Gold does cross the human placenta to a limited degree, and scant deposition occurs in the fetal liver. Rodent studies reveal an increased prevalence of multiple defects involving the CNS, abdominal wall, and limbs.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Gold sodium thiomalate enters human breast milk, and the slow maternal clearance of gold must be remembered. Gold was found in the serum and RBCs of a nursing infant. In one study, the estimated weight-adjusted dose to the infant exceeded that received by the mother.

Pregnancy

. N/V after spinal anesthesia is common and distressing. Granisetron may be superior to both droperidol and metoclopramide for its prevention but controversy continues. The addition of dexamethasone (8mg) further enhances its efficacy. There are several case reports of its use during

Pregnancy

in women receiving chemotherapy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether granisetron crosses the placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether granisetron enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Plasma concentrations of contraceptive steroids are decreased by griseofulvin, which stimulates their hepatic metabolism. Griseofulvin inhibits chromosomal distribution during cell division. Thus, men are cautioned to delay fathering children for 6mo after completing therapy, and women planning conception should wait at least 1mo.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether griseofulvin crosses the human placenta. Epidemiologic studies are limited but reassuring. While teratogenicity is suggested in horses and cats, rodent studies indicating teratogenicity were not confirmed after repetition. There are unsubstantiated reports of an association with conjoined twinning in humans.

Breastfeeding

There are no adequate reports or well-controlled studies of griseofulvin in nursing women. It is unknown whether this drug is excreted in human breast milk.

Pregnancy

. Guaifenesin is a common component in many over-the-counter cough remedies. There are no adequate reports or well-controlled studies in pregnant women. Animal reproduction studies have not been conducted.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether guaifenesin crosses the 459 human placenta. Unfortunately, limited epidemiologic study provides no help in estimating the risk of guaifenesin. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience with guaifenesin in nursing women. It is unknown whether this drug is excreted in human breast milk.

Pregnancy

. There is no published experience with guanabenz during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether guanabenz crosses the placenta. Rodent studies are generally reassuring, with only minor ossification abnormalities noted at doses many multiples of the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether guanabenz enters human breast milk.

Pregnancy

. Guanadrel is an orally active antihypertensive that lowers both systolic and diastolic pressure. It is typically employed as a second-line agent following a diuretic. There is no published experience with guanadrel during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether guanadrel crosses the placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether guanadrel enters human breast milk.

Pregnancy

. This ganglionic blocker is rarely used during pregnancy, as there are other agents with fewer Side effects include hypotension, chest pain, dyspnea, diarrhea, N/V, dry mouth, depression, tremor, blurred vision, weakness, myalgia, dermatitis, weight gain, and increased BUN.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether guanethidine crosses the human placenta. Breastfeeding There are no adequate reports or well-controlled studies in nursing women. Guanethidine does enter human breast milk at very low concentrations.

Pregnancy

. There are no well-controlled trials of guanfacine during pregnancy. It is not generally recommended for the treatment of preeclamptic hypertension, in part because of its slow onset. There is one report of 30 preeclamptic women in which only 24 responded.

Fetal Health

There are no adequate reports or well-controlled studies of guanfacine in human fetuses.

Breastfeeding

There is no published experience in nursing women. It is unknown whether guanfacine enters human breast milk.

Pregnancy

. Haemophilus influenzae conjugate vaccine is a combination of capsular polysaccharides purified from HIB; it protects only against the B strain. There are no adequate reports or well- controlled studies in pregnant women. Maternal immunization does not interfere with subsequent neonatal immunization. Haemophilus influenzae conjugate vaccine is not contraindicated in women with HIV.

Fetal Health

There are no adequate reports or well-controlled studies of H. influenzae conjugate vaccine in human fetuses. The H. influenzae antibodies generated cross the placenta and provide passive immunity. In two studies, it effectively produced passive immunity in the newborn after administration to women during the 3rd trimester. Maternal malnutrition may reduce placental transfer. While animal studies have not been conducted, there is no evidence the vaccine components either cross the placenta or pose a risk to the human fetus.

Breastfeeding

There is no published experience with H. influenzae conjugate vaccine in nursing women. It is certainly possible H. influenzae antibodies enter human breast milk. It is unknown whether they convey any protection to the nursing newborn.

Pregnancy

. There is no published experience with halcinonide during pregnancy. Halcinonide reduces scar formation.

Fetal Health

While there are no adequate reports or well-controlled studies in human fetuses, the quantity of halcinonide absorbed systemically is unlikely to pose a risk to the fetus even if it does cross the placenta. Though some corticosteroids are teratogens in some rodents, there is no substantative evidence they act as teratogens in humans.

Breastfeeding

There is no published experience in nursing women. It is unknown whether halcinonide enters human breast milk. Some nonfluoridated and fluoridated corticosteroids enter human breast milk with M:P ratios ranging between 0.05 and 0.25.

Pregnancy

. There is no published experience with halobetasol during pregnancy. Human and animal studies indicate approximately 2% of the applied cream dose (3% ointment) enters the circulation within 96h of topical administration.

Fetal Health

While there are no adequate reports or well-controlled studies in human fetuses, the quantity of halobetasol absorbed systemically is unlikely to pose a risk to the fetus even if it does cross the placenta. Though some corticosteroids are teratogens in rodents, there is no substantative evidence they act as teratogens in humans. When given systemically to rodents at doses that are multiples of the MRHD, halobetasol is associated with embryotoxicity, cleft palate, and abdominal wall defects.

Breastfeeding

There is no published experience in nursing women. It is unknown whether halobetasol enters human breast milk. Considering the dose and route, it is unlikely the milk concentration will reach a clinically relevant level. Some nonfluoridated and fluoridated corticosteroids enter human breast milk with M:P ratios ranging between 0.05 and 0.25.

Pregnancy

. There are no adequate reports or well-controlled studies of haloperidol in pregnant women. There is, however, a large body of experience during

Pregnancy

suggesting a wide margin of safety. There is 1 case report of an overdose at 34w treated symptomatically without detectable adverse effect. There is another case report of neuroleptic malignant syndrome during

Pregnancy

treated successfully with dantrolene and bromocriptine. Haloperidol has also been used to treat chorea gravidarum. It is similar to olanzapine for the treatment of schizophrenia in terms of compliance, symptoms, extrapyramidal symptoms, and overall quality of life, but haloperidol costs significantly less.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Haloperidol crosses the human placenta (65% of the maternal dose) and can be recovered from neonatal hair. In a series of 188 women who consulted a drug information service after exposure to haloperidol (plus 27 exposed to a similar agent), there was no increase in birth defects, though the preterm birth rate was double that of the matched controls. Two exposed neonates had a limb abnormality. After maternal overdose, the 467 fetus had an abnormal biophysical profile for 5d. Haloperidol is teratogenic in some rodents. In hamsters, it produces a variety of spinal abnormalities in a dose-dependent fashion.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Haloperidol enters human breast milk, and in Breastfeeding infants may reach therapeutic levels. As it is unknown whether haloperidol poses a risk to the neonate,

Pregnancy

. Halothane is a halogenated inhalational agent for which there is a long clinical experience during pregnancy. It and related compounds relax the myometrium both in vitro and in vivo. As a result, it should not be used for routine vaginal delivery. Halothane is no longer used routinely by anesthesiologists, who prefer newer agents that are not significantly metabolized by the liver. Halothane has been used for cesarean delivery and in instances when uterine relaxation is important, such as acute uterine inversion, placental entrapment, and cervical entrapment of the after-coming head during vaginal breech delivery. Currently preferred agents include NO donors.

Fetal Health

Halothane rapidly crosses the human placenta, reaching an F:M ratio approaching unity within minutes. Once considered a candidate anesthetic for fetal surgery, halothane decreases fetal cardiac output and placental blood flow, and increases total vascular resistance in sheep. Placental vascular resistance increases out of proportion to systemic vascular resistance, shunting blood away from the site of gas exchange.

Breastfeeding

There is no published experience in nursing women. It is unknown whether halothane enters human breast milk. Considering the indication, one-time halothane use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Heparin consists of sulfated, long-chain acidic mucopolysaccharides with MWs ranging from 4000 to 30,000 Da. The various LMWHs are derivatives. Each is considered an anticoagulant of choice during pregnancy, is equally effective, and has a similar risk profile. Unfractionated heparin has the principal advantage of low cost. Despite the long history of clinical use, there are no adequate reports or well-controlled studies in pregnant women. Perhaps the greatest clinical limitation is the dose volume that must be used considering the relatively dilute concentrations available. Therapeutic heparinization is the prophylaxis of choice for women with a mechanical heart valve.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Heparin does not cross the placenta, and is not associated with an adverse fetal outcome. However, a recent study suggests that both heparin and LMWH have the potential to reduce trophoblast invasion.

Breastfeeding

There is no published experience in nursing women. It is unknown whether heparin enters human breast milk. 470

Pregnancy

. HAV is a picornavirus, and the vaccine consists of inactivated virus. There are no adequate reports or well-controlled studies in pregnant women. There are no reported adverse effects on mother or fetus. Women either traveling to areas where HAV is endemic, older than 30y with chronic liver disease, waiting for or who have received liver transplants, or working with nonhuman primates should be vaccinated. HAV vaccination of chronic HCV carrier women substantially reduces morbidity and mortality rates. 471 The disease course is typically unaltered by pregnancy, though fulminant hepatitis is reported in the 3rd trimester. Immunoglobulin is a safe alternative for short-term protection.

Fetal Health

There are no adequate reports or well-controlled studies of hepatitis A vaccine in human fetuses. HAV is rarely transmitted to the fetus, and is not a known teratogen. The antibodies produced in response to vaccination are known to cross the placenta and may provide enhanced protection during the neonatal period. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether hepatitis A vaccine enters human breast milk. It is likely the resulting antibodies do enter breast milk, but it is unknown whether they confer any immunity for the nursing newborn. The vaccine is generally considered compatible with breastfeeding.

Pregnancy

. Hepatitis B immune globulin is prepared from pooled plasma. Women who may benefit from inoculation include those exposed to household contacts, an infected sexual partner, and blood from infected individuals. Hepatitis B immune globulin is effective in reducing perinatal transmission of HBV to neonates born to infected women. Though there is controversy on whether the administration of immunoglobulin in the 3rd trimester reduces transmission when given antenatally to Hep Be antigen?positive women, it may be worthwhile. Hepatitis B immune globulin should be administered concomitantly with hepatitis B vaccine. Women previously vaccinated but subsequently exposed should have their immune titers checked immediately, and be covered with immunoglobulin if they are low.

Fetal Health

There are no adequate reports or well-controlled studies of hepatitis B immune globulin in human fetuses. While animal studies have not been conducted, though there is no reason to expect the immunoglobulin to be harmful. Further, administration to susceptible women appears to reduce the incidence of neonatal HBV. Universal vaccination is recommended postnatally.

Breastfeeding

There are no adequate reports or well-controlled studies of hepatitis B immune globulin in nursing women. Vaccinated women have higher immunoglobulin levels in their breast milk.

Pregnancy

. Recombinant vaccines are biotechnologically produced, consisting of nonreplicating antigens. Hepatitis B vaccine appears safe and immunogenic during pregnancy, and immunization may help protect the fetus. Postpartum vaccination is also effective. The number of at-risk patients is large, and many authorities recommend routine vaccination. However, vaccination can usually be delayed until after delivery for most indications. Nonimmune women in geographic locales with high endemic rates benefit from vaccination during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies of hepatitis B vaccine in human fetuses. Passive immunity occurs in more than half of newborns born to women vaccinated during pregnancy. Neonatal vaccination is 95% effective. There does not appear to be any substantative difference among recombinant vaccines. Rodent teratogenicity studies have not been performed, though the native virus is not a known human teratogen.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether hepatitis B vaccine enters human breast milk, but breastfed neonates of vaccinated women have higher hepatitis B antibody levels.

Pregnancy

. Hexachlorophene is not recommended due to narrow spectrum and the risk of percutaneous absorption. A phenol, it can be neurotoxic at high concentrations. While the wound infection rate is reduced after cleansing, and preoperative showers reduce the skin bacterial count, there are better alternatives. There are no adequate reports or well-controlled studies in pregnant women.

Breastfeeding

There is no published experience in nursing women. It is unknown whether hexachlorophene enters human breast milk.

Pregnancy

. Hydralazine is one of the most widely used drug for the treatment of acute hypertension during pregnancy. Women with severe preeclampsia whose intravascular volume is contracted are at risk for hypotension. The risk is ameliorated by the administration of appropriate intravascular volume prior to treatment. It was suggested that the incidence of hypotension is increased by the continuous infusion of hydralazine, but that observation may reflect a variety of other uncontrolled variables such as volume replacement and nursing protocols. Comparative study suggests other commonly used agents, such as nifedipine or labetolol, are equally effective in nulliparas for the control of hypertension with fewer hypotensive complications than hydralazine in multiparas. In one recent randomized trial, mini- bolus doses of diazoxide (15mg) did not cause maternal hypotension as previously described and, compared to hydralazine, produced rapid control and reduced the number of episodes of persistent severe hypertension.

Fetal Health

Hydralazine crosses the human placenta, and the F:M ratio can exceed unity. The impact of the therapeutic level on the human fetus is unknown. Vascular resistance declines in the isolated perfused placenta. Limited use during the 1st trimester reveals no evidence of teratogenicity. The impact of hydralazine on placental blood flow is variable and greatly influenced by the occurrence of hypotension. Rodent studies reveal that hydralazine is teratogenic in mice at 20-30the MRHD and possibly in rabbits at 10-15? the MRHD, but is not teratogenic in rats.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Hydralazine enters human breast milk, but the 476 amount ingested by the Breastfeeding neonate is clinically insignificant.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Low-dose diuretics are the most effective first-line treatment for the prevention of CV disease morbidity 477 and mortality. Hydrochlorothiazide leads to potassium loss and a transient reduction in intravascular volume when first initiated. Thereafter, intravascular volume recovers. Thus, thiazides should not be initiated during

Pregnancy

but may be continued if already in chronic use. These diuretics further reduce an already constricted maternal intravascular volume in women with preeclampsia and should be avoided in such women. Hydrochlorothiazide has been used during

Pregnancy

for the treatment of idiopathic hypoparathyroidism.

Fetal Health

Hydrochlorothiazide crosses the human placenta, achieving an F:M ratio approximating 0.5. It is concentrated in AF. While no evidence of teratogenicity has emerged during the long clinical experience, hydrochlorothiazide can cause neonatal electrolyte abnormalities, thrombocytopenia, and hyperglycemia when given around the time of delivery. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether hydrochlorothiazide enters human breast milk.

Pregnancy

. Hydrocodone is a semisynthetic opioid. Homatropine is included in the formulation at a subtherapeutic level to discourage abuse. There are no adequate reports or well-controlled studies in pregnant women. The analgesia produced by combination with ibuprofen is superior to that achieved with ibuprofen alone. Similar to codeine, it seems more effective for the relief of uterine cramping than episiotomy pain.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Hydrocodone presumably crosses the human placenta. Rodent studies reveal IUGR at doses below those producing maternal toxicity. In an adequate dose, it can cause neonatal depression at birth.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether hydrocodone enters human breast milk. However, codeine and its metabolite morphine are excreted in human breast milk. Breastfeeding neonates have low plasma levels during the first few days of life, in part secondary to the low concentration in milk, and in part due to the small amount of milk produced. Thus, moderate hydrocodone use is probably compatible with breastfeeding. 479

Pregnancy

. Hydrocortisone is a naturally occurring glucocorticoid. Adrenal corticosteroid secretion is increased during pregnancy. There are no adequate reports or well-controlled studies in pregnant women. Case reports suggest

Pregnancy

increases requirements.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Hydrocortisone is inactivated in the placenta. Some glucocorticoids increase the risk of cleft palate in some rodents. There was no increase in registry-type studies in the general frequency of malformations in offspring of women receiving a variety of corticosteroids during pregnancy. Despite placental metabolism, 2g of hydrocortisone administered over 48h in divided doses improves both indices of fetal lung maturity (i.e., L:S ratio) and fetal outcomes compared to no treatment. As such, hydrocortisone is an alternative therapy should either betamethasone or dexamethasone be unavailable for the hastening of lung maturity. It is unknown whether repeated exposure delays myelination as has been reported in animals after either betamethasone or dexamethasone.

Breastfeeding

There is no published experience in nursing women. It is unknown whether hydrocortisone enters human breast milk. Glucocorticoids are a normal component of breast milk. It is not known whether maternal ingestion increases the concentration. The long clinical experience is reassuring.

Pregnancy

. Hydromorphone plus a local anesthetic (e.g., bupivacaine) is popular for epidural anesthesia during labor. Similar to morphine, it enhances the sensory blockade, thus allowing a lower concentration of local anesthetic. The result is a decrease in motor blockade. There are no well-controlled studies of women receiving hydromorphone chronically.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Systemically available hydromorphone rapidly crosses the placenta, achieving an F:M ratio approximating unity. Rodent studies revealed teratogenicity at doses 600the MRHD. 482 Recent study suggests it and other morphine derivatives can reduce total estrogen levels by inhibiting CYP19.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Hydromorphone enters human breast milk. After intranasal administration, the breastfed newborn ingests approximately 0.67% of the maternal dose (adjusted for body weight). Considering the dose and pattern of clinical use, hydromorphone is compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of hydroquinone in pregnant women. There are no indications that require use during pregnancy. Postpartum, it is often used for the treatment of melasma.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Hydroquinone crosses the human placenta and is a teratogen in chicks and some rodents. It can cause hypoploidy in human cell culture lines. Approximately 45-50% of the topically applied dose, or 3mcg/cm2/h, is available for systemic absorption. That said, women who use hydroxyquinone do not experience a detectable increase in adverse

Pregnancy

outcomes.

Breastfeeding

There is no published experience in nursing women. It is unknown whether hydroquinone enters human breast milk. Though the systemic concentration after topical administration is likely to be low, treatment can easily be delayed until weaning.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Hydroxychloroquine reduces serum lipids, including cholesterol, triglycerides, and LDLs. Some recommend discontinuing hydroxychloroquine in pregnant women with connective tissue diseases, even though it has long been used for malarial prophylaxis during

Pregnancy

in malaria-infested areas. In one randomized trial, hydroxychloroquine was associated with a significant reduction in the number of flare episodes in women with SLE. Thus, it may be reasonable to continue the drug considering the terminal elimination t/2 may be up to 2mo, flares of SLE occur after discontinuation, and flares are detrimental to

Pregnancy

outcome.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. While there is no substantive evidence of teratogenicity in rodents, hydroxychloroquine crosses the placenta and is deposited in pigmented fetal tissues. However, several large clinical series in women with either malaria or SLE are reassuring.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. The concentration of hydroxychloroquine entering human breast milk is apparently very low (3.2mcg in breast milk from a woman given 800mg over 48h) and should not pose a threat to the breastfed newborn.

Pregnancy

. There are no adequate reports or well-controlled studies of hydroxyurea in pregnant women. Published experience is limited to case reports and small series of sickle cell disease, thrombocythemia, and leukemia. The beneficial effects of hydroxyurea on sickle cell disease result from an increase in both the intracellular concentration of Hb F and the percentage of Hb F?containing RBCs, improving the hydration and prolonging the life span of the RBCs. In women with essential thrombocythemia, hydroxyurea reduces thrombotic events but does not increase survival. The published clinical experience suggests the risk of hydroxyurea during human

Pregnancy

may be greatly overestimated.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether hydroxyurea crosses the human placenta. Hydroxyurea is embryotoxic and a potent teratogen in a wide variety of animal models. It also causes IUGR 486 and impaired learning in rats. However, the human experience suggests the risk of teratogenicity is somewhat overestimated.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Hydroxyurea enters human breast milk, though the kinetics require further elucidation. Considering it is a potent mutagen, hydroxyurea should perhaps be avoided while Breastfeeding until there is additional information available.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Hydroxyzine remains a first-line agent for the treatment of pruritus and nausea during pregnancy. It is often administered with narcotic agents to reduce the frequency of nausea. Hydroxyzine reduces the pruritus associated with epidural or spinal morphine and morphine analogs. Hydroxyzine is superior to droperidol for relief of nausea associated with general anesthesia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether hydroxyzine crosses the human placenta, though its administration is associated with a significant decrease in FHR variability when administered during labor. Epidemiologic studies of women taking hydroxyzine for allergy symptoms are reassuring. There is a single case report of neonatal seizures associated with hydroxyzine withdrawal after chronic intrauterine exposue. In rodents, high doses of hydroxyzine are associated with an increased rate of malformations.

Breastfeeding

There is no published experience in nursing women. It is unknown whether hydroxyzine enters human breast milk.

Pregnancy

. There is no published experience with hyoscyamine during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Hyoscyamine reportedly crosses the human placenta. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. Trace amounts of hyoscyamine are excreted into human breast milk, though the kinetics remain to be elucidated.

Pregnancy

. About 5% of women report prenatal use of either ibuprofen or naproxen near conception or during pregnancy. In several different trials, the addition of hydrocodone significantly enhanced the analgesic efficacy of ibuprofen. In other trials, ibuprofen significantly reduced postabortal pain and was superior to acetaminophen for the treatment of postpartum pain and episiotomy after vaginal delivery. Prophylactic ibuprofen does not decrease the discomfort associated with IUD insertion. In one 490 prospective case-control study, prenatal ibuprofen or naproxen use increased the risk of spontaneous abortion by 80% (adjusted hazard ratio 1.8 [95% CI 1.0-3.2]). The association was stronger if the initial use was around conception or if it lasted more than a week. There is epidemiologic evidence linking it to PPH.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Ibuprofen crosses the human placenta and is found in meconium. Fetal levels are dependent on maternal, as NSAID agents are not metabolized by the fetal kidney. Constriction of the fetal ductus arteriosus is reported, and it is similar in efficacy to indomethacin for closure of a neonatal PDA. There is epidemiologic evidence linking ibuprofen to gastroschisis. Similar adverse effects have been noted in rats where ibuprofen was associated with an increased prevalence of abdominal wall defects and VSD. Ibuprofen is as effective as indomethacin in closing the ductus arteriosus, but does not affect renal function to the same extent. In cows, ibuprofen actually enhances the rate of implantation.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only small amounts of ibuprofen are excreted into human breast milk. Less than 1mg is excreted in the breast milk of lactating women who ingest up to 400mg q6h.

Pregnancy

. There are no adequate reports or well-controlled studies of ibutilide in pregnant women. The published experience is limited to case reports and short series. Its efficacy is apparently uncompromised by pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Class III antiarrhythmic drugs such as ibutilide cause a spectrum of malformations in experimental teratology studies very similar to those reported for phenytoin. Class III antiarrhythmics decrease cardiac cell excitability by selectively blocking the rapid component of the IKr, an action shared with phenytoin. Malformations associated with selective and nonselective IKrblockers may be the dose-dependent product of embryonic bradycardia/arrhythmia resulting in (1) hypoxia, explaining embryonic death and growth restriction; (2) episodes of severe hypoxia, followed by generation of reactive oxygen species within the embryo during reoxygenation, causing orofacial clefts and distal digital reductions; and (3) alterations in embryonic blood flow and BP, inducing CV defects.

Breastfeeding

There is no published experience in nursing women. It is unknown whether ibutilide enters human breast milk. 492

Pregnancy

. Idarubicin is an analog of daunorubicin. There are no adequate reports or well-controlled studies in pregnant women. The published experience is limited to case reports and short series. Its efficacy is apparently uncompromised by pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Idarubicin apparently crosses the human placenta, as there are multiple case reports of fetal cardiotoxicity usually in the setting of polypharmacy. Idarubicin is embryotoxic and teratogenic in rodents at a fraction of the MRHD. 493

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether idarubicin enters human breast milk. However, considering its mechanism of action, it is perhaps best to avoid Breastfeeding while idarubicin is administered.

Pregnancy

. There is no published experience with idoxuridine during pregnancy. The quantity of drug absorbed systemically is unknown.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether idoxuridine crosses the human placenta. Rodent studies reveal evidence of teratogenicity and embryotoxicity after systemic administration.

Breastfeeding

There is no published experience in nursing women. It is unknown whether idoxuridine enters human breast milk.

Pregnancy

. Imipenem-cilastin is broad-spectrum combination that achieves excellent pelvic tissue levels. Because of the relatively high cost, it is not considered ??first-line?? therapy for most obstetric and gynecologic infections. There are no adequate reports or well- controlled studies in pregnant women. The clearance of imipenem-cilastin is increased during pregnancy. Limited study reveals good clinical responses in women with chorioamnionitis or PPROM. While imipenem-cilastin provides effective prophylaxis for women undergoing nonelective cesarean delivery, it is no better than any other antibiotic agent used for this purpose. The selection of an agent for cesarean section prophylaxis typically is based on cost.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Imipenem-cilastin crosses the human placenta, achieving an F:M ratio of only 0.3, while the AF:F ratio is 0.6. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Adverse outcomes in animal studies share an association with adverse maternal outcomes.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Limited concentrations of imipenem-cilastin are excreted into human breast milk, though the kinetics remain to be elucidated. It is generally considered compatible with breastfeeding.

Pregnancy

. Depression is common during and after

Pregnancy

but often goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. Imipramine is the prototype TCA and is predominantly metabolized by hepatic CYP2D6. There are no adequate reports or well-controlled studies in pregnant women. It has been used extensively during

Pregnancy

for the treatment of depression. Imipramine has also been used during

Pregnancy

for the treatment of panic attack.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Imipramine binds to the placental serotonin 496 transporter, and presumably crosses the human placenta. It rapidly crosses the rodent placenta and is distributed throughout the fetus. While rodent teratogenicity studies are generally reassuring, several behavioral studies suggest prenatal exposure to imipramine alters postnatal adrenergic responses, serotonin uptake, and the response to stress.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Imipramine is excreted into human breast milk, though the kinetics remain to be elucidated. It is estimated that, in women ingesting therapeutic doses of imipramine, the infant would ingest 0.2mg/L, or 30mcg/kg/d. Only about 3% of the maternal dose (per kg) of other tricyclics is consumed by the breastfed neonate.

Pregnancy

. The published experience with imiquimod during

Pregnancy

is limited to case reports. There are no studies of systemic absorption.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether imiquimod crosses the human placenta. Imiquimod does not stimulate inflammatory cytokines when applied to cultured trophoblasts. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no experience in nursing women. However, it is unlikely, considering the dose and route, that any significant concentration of imiquimod enters human breast milk.

Pregnancy

. IV immune globulin (human) is a solvent/detergent treated, sterile, freeze-dried preparation of highly purified IgG derived from large pools of human plasma. The manufacturing process dramatically reduces the risk of viral transmission. The t/2 of immune globulin approximates 38d. Epinephrine should be available for treatment of any acute anaphylactic reactions. There are few well-controlled studies in pregnant women, but several on- and off-label indications deserve specific comment. In addition to the indications listed below, immune globulin has been used with apparent success during

Pregnancy

for dermatomyositis, Churg-Strauss vasculitis, Guillain-Barre? syndrome, and acquired hemophilia A. ITP: ITP is a common hematologic disorder in young women. While ITP is a risk to both mother and neonate, there is no 499 convincing evidence it poses a risk to the fetus. Cesarean delivery is not indicated for ITP. Alloimmune thrombocytopenia: It is now clear that maternal immune globulin therapy is primary treatment for fetal alloimmune thrombocytopenia. Empiric therapy (i.e., treatment of at-risk fetuses without a definitive diagnosis) is cost-effective. A high-dose weekly infusion (1-3g/kg) reduces the severity of fetal alloimmune thrombocytopenia and the risk of a fetal intracranial hemorrhage. The concurrent use of dexamethasone is not of added value, though nonresponders to immune globulin may benefit from the addition of prednisone 60mg PO qd. The mechanism is unknown. Maternal sera obtained after treatment with polyclonal immunoglobulin decrease constitutive and cytokine-induced ICAM-1 and VCAM-1 expression on endothelial cells. The initial fetal platelet count predicts the response to therapy, but apparently not the family history. Children with fetal alloimmune thrombocytopenia treated as fetuses have better long-term developmental-behavioral outcomes than untreated siblings, perhaps because of higher in utero platelet counts. RBC alloimmunization: A number of pregnancies have been reported noting favorable outcomes with immune globulin (1-2g/ kg qw) treatment of women with severe Rh factor disease, though that conclusion is not unanimous. Several combine immune globulin therapy with plasmapheresis. One explanation for an improved outcome would be decreased hemolysis. In support, several groups document either a decreased need for transfusion or a reduced carboxyhemoglobin level in rH factor?immunized neonates after immune globulin therapy. While therapy does not typically eliminate the need for fetal transfusion, it does appear to delay the gestation in which it must be started. Recurrent abortion: The use of immune globulin in women with recurrent

Pregnancy

loss remains controversial. In a recent meta- analysis, immune globulin was ineffective for the indication of primary recurrent abortion, but was associated with an increased the rate of live births in women with secondary recurrent miscarriage.

Fetal Health

There are no adequate and well-controlled studies in human fetuses. Animal reproduction studies have not been conducted. IV immune globulin crosses the human placenta via the Fc0 receptors on the syncytiotrophoblast, as do endogenous immunoglobulins. However, not all commercial preparations have equal transport. Using an in vitro placental perfusion model, there was significant inhibition of placental anti-D IgG transfer with three commercial immune globulin preparations where the circulating maternal IgG concentrations were >20g/L. One product, which was not inhibitory, had lower circulating IgG levels (16.5 ? 0.9g/L) and significantly reduced placental transfer of total IgG, suggesting that the reduced functional activity of IgG from immune globulin preparations may correlate with poor clinical efficacy.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether immune globulin enters human breast milk, though endogenous immunoglobulins are a normal component of breast milk. 500

Pregnancy

. There is no published experience with indapamide during pregnancy. Diuretics should not be used for the treatment of physiologic edema during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether indapamide crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. However, other thiazide diuretics have neonatal sequelae.

Breastfeeding

There is no published experience in nursing women. It is unknown whether indapamide enters human breast milk.

Pregnancy

. Indinavir is effective reducing the maternal HIV viral load to an undetectable level, especially when combined with other agents such as a nucleoside analog or a reverse transcriptase inhibitor. In one study of 4 women, clearance was increased during

Pregnancy

as reflected in the decreased AUC. In another longitudinal study, indinavir AUC was 68% lower antepartum compared to postpartum, suggesting increased intestinal and/or hepatic CYP3A activity during pregnancy.

Fetal Health

Indinavir crosses the human placenta, though the magnitude of fetal-to-maternal transfer in the isolated cotyledon is 2-3greater than maternal-to-fetal transfer, suggesting fetal exposure is minimal. Transport is via P-glycoprotein. These in vitro findings are confirmed by umbilical cord blood samples. In one series, the majority of pregnancies treated had some adverse outcome, though the relationship of the retroviral therapies to the outcome was unclear. Certainly, the prevention of HIV transmission remains the ultimate priority. Though most premarketing rodent teratogenicity studies are reassuring, indinavir was associated in one study with delayed growth, and skeletal and ophthalmic abnormalities.

Breastfeeding

There is no adequate experience in nursing women. Indinavir does enter human breast milk, and in a single case the M:P ratio was 5.4. It is excreted into rat breast milk. Regardless, Breastfeeding is contraindicated in HIV-infected nursing women 503 where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. Indomethacin is used off-label for the treatment of presumed preterm labor. In that scenario, it significantly prolongs gestation (48-72h), a degree similar to b-mimetic agents and, in small trials, magnesium sulfate. The latter is relevant since in meta-analyses magnesium sulfate is no better than placebo for tocolysis. The interval is adequate for the administration of corticosteroids to enhance fetal lung maturity. Indomethacin is no better and likely inferior to calcium channel blockers such as nifedipine, which has a stronger safety profile. Continuing indomethacin after the successful treatment of presumed preterm labor does not further delay delivery or enhance outcome and should not be condoned. Similarly, indomethacin is advocated for the treatment of the sonographically detected short cervix. Here, too, there is little quality evidence to support the practice. It does not appear to delay preterm delivery of women with a dilated cervix independent of cerclage. Indomethacin has multiple non?prostaglandin-related actions, including the inhibition of MMPs 2 and 9 in amnion, chorion, and decidua. Such actions may contribute to its 505 anti-inflammatory effect. Indomethacin reduces renal free water clearance and can cause abrupt maternal weight gain and edema when first initiated. Indomethacin should probably be avoided in women at risk for delivery within 24h, as a 50mg dose reproducibly prolongs the maternal bleeding time, in half of which cases will reach abnormal levels.

Fetal Health

Indomethacin crosses the placenta, and fetal sequelae are common. Fetal levels are dependent on maternal, as NSAIDs are not metabolized by the fetal kidney. A third of fetuses exposed to indomethacin for 1w or more develop oligohydramnios or evidence of ductal constriction. These adverse effects are completely avoidable as there are no demonstrable benefits over the long term for the indication of preterm labor or incompetent cervix. Other prostaglandin synthase inhibitors reputedly have a lower incidence of fetal sequelae when used as a tocolytic agent, though the quantity of clinical experience is much smaller than that for indomethacin. These differences are clear in the neonate when comparing ibuprofen to indomethacin for the closure of a PDA. Because of its effect on fetal urine output, indomethacin is used to treat idiopathic polyhydramnios. It should not, however, be used in twin gestations complicated by the so-called stuck twin, or the ??oligo-polyhydramnios sequence.?? In this scenario, there is no evidence that indomethacin prolongs gestation, and it can lead to fetal renal shutdown. The effects of indomethacin on the fetal kidneys are dose- and duration-dependent. Stopping it typically results in reversal of the abnormal sonographic findings. Indomethacin is used postnatally for the pharmacologic closure of a PDA. Constriction of the fetal ductus is common when indomethacin is used for the treatment of preterm labor. It, too, reverses with cessation, and the long-term impact of in utero ductal constriction on the otherwise healthy fetus is currently unknown. A short course (<48h) of indomethacin for the treatment of preterm labor does not alter the newborn?s responsiveness to indomethacin postnatally. In uncontrolled trials, indomethacin tocolysis was associated with an increased risk of IVH and NEC in the neonate. These reports remain to be confirmed. In other uncontrolled studies, neurodevelopment was unaffected by antenatal exposure.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. The quantity of indomethacin excreted into human breast milk is low, such that the breastfed neonate would ingest <1% of the maternal dose per day. Neonatal plasma levels are typically below detection.

Pregnancy

. There are no adequate reports or well-controlled studies of infliximab use during pregnancy. The current experience is limited to case reports and small series.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It appears that infliximab crosses the human placenta. Limited case reports are reassuring. Rodent teratogenicity studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Infliximab is a high-MW antibody. No drug was detected in 2 women studied over multiple time points.

Pregnancy

. All pregnant women >12w gestation should be vaccinated in preparation for influenza season. Pregnant women have increased susceptibility to viral respiratory diseases, and the most common one is influenza. Influenza-associated excess mortality during

Pregnancy

was documented during the pandemics of 1918-1919 and 1957-1958. The increased risk might result from (1) increased HR, stroke volume, and oxygen consumption; (2) decreased lung capacity; and (3) changes in immunologic function. A study during 17 interpandemic influenza seasons revealed that the relative risk for hospitalization for cardiorespiratory conditions during

Pregnancy

increased from 1.4 between 14 and 20w gestation to 4.7 between 37 and 42w 509 gestation, compared to women 1-6mo postpartum. Researchers estimate that an average of 1-2 hospitalizations can be prevented for every 1000 pregnant women vaccinated. Thus, all women who intend to become pregnant or are pregnant should receive the influenza vaccine. Vaccination can occur in any trimester. One study of influenza vaccination of >2000 pregnant women demonstrated no adverse fetal effects associated with influenza vaccine. If a pregnant woman develops influenza, she should be treated with supportive care. Antiviral medications should be reserved for cases where the benefits outweigh the risks.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether influenza vaccine crosses the human placenta. Vaccine-stimulated IgG crosses the placenta, perhaps conveying some degree of passive immunity, and it was recently reported that B- and T-cell immune responses occur in the fetus after influenza vaccination. Maternal influenza vaccination reduces respiratory illness rates in their infants by almost2=3 up to 6m of age. There is no evidence heat-killed vaccine is teratogenic if given in the 1st trimester. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether influenza vaccine enters human breast milk. It is likely the stimulated maternal IgG is excreted into the breast milk.

Pregnancy

. Insulin aspart is a rapid-acting human insulin analog whose onset is roughly twice as fast as regular human insulin. It is similar to insulin lispro, which is similar to regular human insulin in controlling postprandial hyperglycemia without increasing the risk of hypoglycemia. Insulin aspart has an added advantage over regular human insulin in that it can be taken immediately before the meal, rather than 30-60min before. One recent and well-powered RCT concluded that insulin aspart is at least as safe and effective as regular human insulin when used in basal-bolus therapy with neutral protamine Hagedorn (NPH) insulin in pregnant women with type 1 diabetes, and may potentially offer some benefits in terms of postprandial glucose control and preventing severe hypoglycemia. Careful monitoring of glucose levels coupled with active regulation of the insulin dose is crucial for an optimal outcome.

Fetal Health

Insulin does not cross the placenta. Hyperglycemia is associated with both an embryopathy and fetopathy. Women with insulin- requiring diabetes pre

Pregnancy

are at increased risk of bearing a child with a structural malformation. The magnitude of the risk correlates directly with the overall degree of hyperglycemia. Normalization of glucose prior to conception lowers the risk below that of control populations. Euglycemia after the embryonic stage prevents the diabetic fetopathy. While rodent 511 teratogenicity studies revealed increased early

Pregnancy

losses, these were likely the product of severe hypoglycemia.

Breastfeeding

There is no published experience in nursing women. It is unknown whether insulin aspart enters human breast milk. Human insulin is a normal component of breast milk. A wide body of clinical experience with similar insulin preparations suggests it will be compatible with breastfeeding. Lactating women may require dose or meal adjustments or both.

Pregnancy

. Insulin glargine is a long-acting recombinant insulin analog. There are no adequate reports or well-controlled studies in pregnant women. The published expereince is confined to case reports and small series. Though the fact that insulin requirements can change dramatically between 16 and 30w gestation, one might intuit the long-acting profile of insulin glargine renders it a poor choice for acute management. However, the case reports suggest it may work well for the basal release of insulin between meals. Careful monitoring of glucose levels coupled with active regulation of the insulin dose is crucial for an optimal outcome.

Fetal Health

There are no adequate reports or well-controlled studies of insulin glargine in human fetuses. Insulin does not cross the placenta. Hyperglycemia is associated with both an embryopathy and fetopathy. Women with insulin-requiring diabetes pre

Pregnancy

are at increased risk of bearing a child with a structural malformation. The magnitude of the risk correlates directly with the overall degree of hyperglycemia. Normalization of glucose prior to conception lowers the risk below control populations. Euglycemia after the embryonic stage prevents the diabetic fetopathy. While rodent teratogenicity studies revealed increased early

Pregnancy

losses, these were likely the product of severe hypoglycemia.

Breastfeeding

There is no published experience in nursing women. It is unknown whether insulin glargine enters human breast milk. Human insulin is a normal component of breast milk. A wide body of clinical experience with similar insulin preparations suggests it will be compatible with breastfeeding. Lactating women may require dose or meal adjustments or both.

Pregnancy

. Insulin lispro is a rapid-acting human insulin analog with the same potency as regular human insulin. In nonpregnant patients, insulin lispro is superior to regular human insulin for the control of postprandial hyperglycemia without increasing the risk of hypoglycemia. Insulin lispro has an added advantage over regular human insulin that it can be taken immediately before the meal, rather than 30-60min before. The published experience suggests that similar

Pregnancy

outcomes are obtained with fewer hypoglycemic episodes compared to regular human insulin. Though there are no adequate reports or well-controlled studies in pregnant women, many state that either this agent or insulin aspart should replace regular human insulin in combination with a long-acting insulin because of a more physiologic release profile. Careful monitoring of glucose levels coupled with active regulation of the insulin dose is crucial for an optimal outcome.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Native insulin and insulin lispro, specifcally, do not cross the human placenta. Hyperglycemia is associated with both an embryopathy and fetopathy. Women with insulin- requiring diabetes pre

Pregnancy

are at increased risk of bearing a 514 child with a structural malformation. The magnitude of the risk correlates directly with the overall degree of hyperglycemia. Normalization of glucose prior to conception lowers the risk below control populations. Euglycemia after the embryonic stage prevents the diabetic fetopathy. While rodent teratogenicity studies revealed increased early

Pregnancy

losses, these were likely the product of severe hypoglycemia.

Breastfeeding

There is no published experience in nursing women. It is unknown whether insulin lispro enters human breast milk. Human insulin is a normal component of breast milk. A wide body of clinical experience with similar insulin preparations suggests it will be compatible with breastfeeding. Lactating women may require dose or meal adjustments or both.

Pregnancy

. Native insulin is isolated from the porcine pancreas and modified to produce three additional compounds with differing absorption patterns. Although it was the mainstay of diabetes therapy for decades, most diabetic patients begin therapy or switch to therapy with a human insulin analog. Careful monitoring of glucose levels coupled with active regulation of the insulin dose is crucial for an optimal outcome. An insulin infusion may be desirable at times during hospitalization. A basal rate can be provided with regular insulin (100U/100ml) infused at a rate 0.55-1.5U/h.

Fetal Health

There are no adequate reports or well-controlled studies of porcine insulin in human fetuses. Insulin does not cross the placenta. Hyperglycemia is associated with both an embryopathy and fetopathy. Women with insulin-requiring diabetes pre

Pregnancy

are at increased risk of bearing a child with a 516 structural malformation. The magnitude of the risk correlates directly with the overall degree of hyperglycemia. Normalization of glucose prior to conception lowers the risk below control populations. Euglycemia after the embryonic stage prevents the diabetic fetopathy. While rodent teratogenicity studies revealed increased early

Pregnancy

losses, these were likely the product of severe hypoglycemia.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether porcine insulin enters human breast milk. Human insulin is a normal component of breast milk. A wide body of clinical experience with similar insulin preparations suggests it will be compatible with breastfeeding. Lactating women may require dose or meal adjustments or both.

Pregnancy

. Human recombinant insulin is synthesized from bacteria containing the human insulin gene. It is then modified to produce three additional compounds with differing absorption patterns. There is a large body of clinical experience using human recombinant insulin during pregnancy. Careful monitoring of glucose levels coupled with active regulation of the insulin dose is crucial for an optimal outcome. An insulin infusion may be desirable at times during hospitalization. A basal rate can be provided with regular insulin (100U/100ml) infused at a rate 0.55-1.5U/h.

Fetal Health

Insulin does not cross the placenta. Hyperglycemia is associated with both an embryopathy and fetopathy. Women with 518 insulin-requiring diabetes pre

Pregnancy

are at increased risk of bearing a child with a structural malformation. The magnitude of the risk correlates directly with the overall degree of hyperglycemia. Normalization of glucose prior to conception lowers the risk below control populations. Euglycemia after the embryonic stage prevents the diabetic fetopathy. While rodent teratogenicity studies revealed increased early

Pregnancy

losses, these were likely the product of severe hypoglycemia.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether human recombinant insulin enters human breast milk. Human insulin is a normal component of breast milk. A wide body of clinical experience with similar insulin preparations suggests it will be compatible with breastfeeding. Lactating women may require dose or meal adjustments or both.

Pregnancy

. Human semisynthetic insulin is synthesized from purified pork insulin, and then enzymatically modified to the human structure. It is functionally the same as regular human insulin. There are no published reports of its use during

Pregnancy

or lactation. Careful monitoring of glucose levels coupled with active regulation of the insulin dose is crucial for an optimal outcome.

Fetal Health

There are no adequate reports or well-controlled studies of human semisynthetic insulin in human fetuses. Insulin does not cross the placenta. Hyperglycemia is associated with both an embryopathy and fetopathy. Women with insulin-requiring diabetes pre

Pregnancy

are at increased risk of bearing a child with a structural malformation. The magnitude of the risk correlates directly with the overall degree of hyperglycemia. Normalization of glucose prior to conception lowers the risk below control populations. Euglycemia after the embryonic stage prevents the diabetic fetopathy. While rodent teratogenicity studies revealed increased early

Pregnancy

losses, these were likely the product of severe hypoglycemia.

Breastfeeding

There is no published experience in nursing women. It is unknown whether human semisynthetic insulin enters human breast milk. Human insulin is a normal component of breast milk. A wide body of clinical experience with similar insulin preparations suggests it will be compatible with breastfeeding. Lactating women may require dose or meal adjustments or both.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Case reports document the use of interferon alfa-2a during

Pregnancy

to treat essential thrombocythemia, CML, and chronic HCV infection. A decrease in serum estradiol and progesterone levels is reported in women receiving human leukocyte interferon.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. The risk of HCV vertical transmission is estimated to approximate 5%. Interferon alfa-2a does not cross the isolated perfused human placenta. There is a single case report of a preterm birth associated with IUGR and neonatal lupus-like syndrome. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. However, it increases the risk of abortion when given at multiples of the MRHD to rhesus monkeys early in gestation. There is no detectable effect in late gestation.

Breastfeeding

There is no published experience in nursing women. It is unknown whether interferon alfa-2a enters human breast milk. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission. 521

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Case reports document the use of interferon alfa-2b during

Pregnancy

for the treatment of chronic HCV 522 infection and essential thrombocythemia. HIV infection is not a contraindication to HCV infection therapy. Liver disease caused by chronic HCV infection is the second leading cause of death in some HIV-infected populations.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether interferon alfa-2b crosses the placenta, though other interferons do not. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. However, it increases the risk of abortion when given at multiples of the MRHD to rhesus monkeys early in gestation.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Only a scant quantity of interferon alfa-2b enters human breast milk. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. Interferon alfa-N3 is derived from human leukocytes. There is no published experience with interferon alfa-N3 during pregnancy. It had no effect on the menstrual cycle of treated, nonpregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether interferon alfa-N3 crosses the placenta, though other interferons do not. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether interferon alfa-N3 enters human breast milk.

Pregnancy

. Interferon alfacon-1 is a non?naturally occurring recombinant type-I interferon. There is no published experience during pregnancy. 524

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether interferon alfacon-1 crosses the human placenta, though other interferons do not. While rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically, there is an increase in embryonic loss in both rodents and some monkeys.

Breastfeeding

There is no published experience in nursing women. It is unknown whether interferon alfacon-1 enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of interferon beta-1a in pregnant women. The relapse rate of MS decreases during

Pregnancy

and increases postpartum. Menstrual irregularities occurred in monkeys treated with 100the MRHD. Anovulation and decreased serum progesterone levels were also noted transiently in some animals. These effects are reversible by discontinuing the drug. Treatment with twice the recommended weekly dose had no effect on cycle duration or ovulation.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether interferon beta-1a crosses the placenta; other interferons do not. Limited study suggests an increase in the rates of

Pregnancy

wastage and IUGR. There was no evidence of teratogenicity in either rodent or monkey studies. However, it was embryolethal or an abortifacient in cynomolgus monkeys administered doses approximately twice the cumulative weekly human dose either during organogenesis or later in pregnancy.

Breastfeeding

There is no published experience in nursing women. It is unknown whether interferon beta-1a enters human breast milk.

Pregnancy

. There are not adequate reports or well controlled studies of interferon beta-1b during pregnancy. The relapse rate of MS decreases during

Pregnancy

and increases postpartum. Menstrual irregularities occur in monkeys treated with 100the MRHD. Anovulation and decreased serum progesterone levels were also 526 noted transiently in some animals. These effects reversed after stopping the drug. Treatment with twice the recommended dose had no effect on cycle duration or ovulation.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether interferon beta-1b crosses the human placenta; other interferons do not. Limited study suggests an increase in the rates of

Pregnancy

wastage and IUGR. There is no evidence of teratogenicity in either rodent or monkey studies. However, there was a significant increase in embryolethal and abortifacient effects in cynomolgus monkeys treated with twice the weekly human dose.

Breastfeeding

There is no published experience in nursing women. It is unknown whether interferon beta-1b enters human breast milk.

Pregnancy

. There is no published experience with interferon gamma-1b during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether interferon gamma-1b crosses the human placenta; other interferons do not. Studies in pregnant primates treated with intravenous doses 2-100the MRHD revealed no teratogenic activity. However, interferon gamma-1b increased the incidence of abortion in primates given 100the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether interferon gamma-1b enters human breast milk.

Pregnancy

. Acarbose is the subject of a large ongoing trial to determine whether its use can reduce or delay the onset of type II diabetes in patients with impaired glucose intolerance. The preliminary results indicate benefit. There are no adequate reports or well-controlled studies of acarbose in pregnant women. There is a single report of 6 pregnant women with impaired glucose tolerance treated with acarbose. Glucose levels returned to normal, and the pregnancies were reportedly uncomplicated.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Only 2% of the oral dose is absorbed. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses almost 10higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether acarbose enters human breast milk. A single rat study suggests acarbose might alter the composition of breast milk by inhibiting lipogenesis. Less than 2% of acarbose is bioavailable. It is unlikely any would be excreted into the milk and or absorbed by the neonate.

Pregnancy

. There are no adequate reports or well-controlled studies of acebutolol in pregnant women. Acebutolol was significantly less successful than either labetalol or a-methyldopa in controlling chronic arterial hypertension >90mmHg in one small randomized trial. The rates of

Pregnancy

complications among the 3 groups of women were similar.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Acebutolol and its main metabolite, N-acetylacebutolol, cross the placenta with a 0.6:0.8 M:F ratio. A prospective study of acebutolol?s hemodynamic and renal impact on neonates after chronic in utero exposure found hemodynamic failure in 5/11 children delivered of treated mothers. Exposed neonates had significantly less early neonatal diuresis, absence of a significant rise in the GFRs, and reduced sodium and calcium balances. The direct effect of the drug on the glomerular and tubular functions and/or the renal arteriolar vasomotoricity could explain these effects. 2

Breastfeeding

Acebutolol and N-acetylacebutolol are concentrated in breast milk (M:P ratios 2:9 for acebutolol and 2:25 for N-acetylacebutolol), though symptoms of neonatal b-blockade are rarely reported. A neonate might receive pharmacologically active amounts of acebutolol if the daily maternal dosage exceeds 400mg and/or renal function in the mother is impaired. However, the American Academy of Pediatrics considers acebutolol permissible with breastfeeding.

Pregnancy

. Acetaminophen is component of a long list of OTC medications. It is metabolized in the liver and excreted by the kidneys. During the 1st trimester, the mean t/2 is significantly lower and oral clearance is significantly higher compared to nonpregnant control subjects. Only during

Pregnancy

is weight related to clearance, 4 suggesting the dose may need to be adjusted in obese women. Ibuprofen provides more rapid relief of perineal pain after vaginal delivery. Up to2=3 of pregnant women ingest acetaminophen some time during gestation. In one recent RCT, acetaminophen plus oxycodone was superior to patient- controlled morphine for the relief of post-cesarean pain. There are no obvious differences in clearance at term. Chronic abuse and overdose are the most common problems. The damage appears secondary to free radical toxicity with consumption of glutathione. N-acetylcysteine is the treatment of choice for acute overdose. In one prospective case-control study, use of prenatal ibuprofen, naproxen, and aspirin, but not acetaminophen, increased the risk of spontaneous abortion by 80% (adjusted hazard ratio 1.8 [95% CI 1.0-3.2]). The association was stronger if the initial use occurred around conception or if the use lasted more than a week.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Acetaminophen crosses the human placenta, reaching steady state in the isolated perfused model within 1h. The F:M ratio for acetaminophen approximated 0.12 in the pregnant ewe, and neither sulfate or glucuronide metabolites crossed. Acetaminophen use during labor to treat the fever of chorioamnionitis is associated with improved fetal umbilical blood gases, presumably by reducing fetal oxygen demand as the maternal core temperature declines. Although it was previously suggested that exposure to acetaminophen was associated with clubfoot and digital abnormalities, these reports are not sustained in large series. However, there appears to be a link between it and gastroschisis and small bowel atresia, but not cardiac ventriculoseptal defects. Unlike aspirin, acetaminophen has no antiplatelet activity and does not pose a hemorrhagic risk to the fetus.

Breastfeeding

Acetaminophen is excreted in low concentrations into breast milk. The amount of the drug administered to the mother estimated to be available to the neonate ranges from 0.04% to 0.23%, and it is generally considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of acetazolamide in pregnant women.

Pregnancy

is not known to alter the impact, efficacy, and dosing of acetazolamide.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Acetazolamide apparently crosses the human placenta. There is no suggestion of teratogenicity in humans despite a long clinical experience. A single case report documents a preterm infant whose mother was treated for glaucoma throughout

Pregnancy

with oral acetazolamide. When renal tubular acidosis developed, acetazolamide was detected in the child?s serum, confirming transplacental passage. In some rodents, acetazolamide is teratogenic (skeletal abnormalities consisting variably of ossification defects or some form of postaxial forelimb ectrodactyly in rats, urinary malformations in mice when combined with amiloride). The prevalence of defects is enhanced when combined with ibuprofen.

Breastfeeding

Acetazolamide is not concentrated in the milk, and the neonatal exposure is <0.5% of the maternal dose. It is generally considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of acetohexamide in pregnant women, and no publications within the last 3 decades. Some oral hypoglycemic drugs are associated with an increased risk of CV death compared to diet and insulin control of glucose.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Although acetohexamide apparently crosses the placenta, there are no reports of teratogenicity in humans. Prolonged neonatal hypoglycemia associated with hyperinsulinism is reported. Differences in the extent of the placental transport of various sulfonylureas are reported. Embryotoxicity is noted in rodent studies.

Breastfeeding

There is no published experience in nursing women. It is unknown whether acetohexamide enters human breast milk as other sulfonylureas do.

Pregnancy

. N-acetylcysteine is a prototype antioxidant presently used nearly exclusively during

Pregnancy

for the treatment of maternal drug toxicity associated with free radical excess such as that occurring with acetaminophen. There are no adequate reports or well- controlled studies of N-acetylcysteine in pregnant women. It has been used for the treatment of acetaminophen toxicity during pregnancy. N-acetylcysteine or another like compound may have a role in the treatment of several disorders associated with excess free radical generation, including preterm labor and preeclampsia. For example, its administration reduced maternal hypertension after uterine artery ligation in rats.

Fetal Health

N-acetylcysteine crosses the placenta, reaching equilibrium with maternal sera. In laboratory studies, it reduces embryo toxicity associated with hyperglycemia, hypoxia, and sepsis. In other studies, it reduces the adverse fetal effects of maternal inflammation by in part blocking the inflammation-stimulated release of cytokines. More recently, it has been shown to prevent neuronal loss in chronically hypestemic guinea pig fetuses.

Breastfeeding

There is no published experience in nursing women. It is unknown whether N-acetylcysteine enters human breast milk. It is unlikely short-term administration for an acute problem would pose a risk to the nursing infant.

Pregnancy

. Treatment is not curative, but rather intended to reduce the duration of symptoms and viral shedding. There is a long clinical experience free of obvious adverse effects. A recent meta-analysis concluded that prophylactic acyclovir beginning at 36w reduced the risks of clinical recurrence of genital herpes at delivery, cesarean section for recurrence, and herpes shedding at delivery. Suppression therapy is both effective and cost-effective whether or not the primary infection occurred during the current pregnancy. Because acyclovir is excreted via the kidneys, its t/2 may be reduced during pregnancy, but this has not been studied specifically. Its combination with zidovudine alters the clearance of both agents in pregnant rats.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether acyclovir crosses the human placenta. It is unclear whether maternal prophylaxis reduces the incidence of neonatal herpes. Post-marketing surveillance by Glaxo-Wellcome has not revealed any increase in or pattern of malformations after acyclovir exposure during the 1st trimester (756 pregnancies). A recent population-based study fromthat included 90 systemic and 995 topical exposures was likewise reassuring. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Acyclovir is passively secreted and achieves concentrations in breast milk higher than maternal serum, and is used to treat neonatal herpetic infection. It is generally considered compatible with breastfeeding. It has been estimated that the unsupplemented newborn would ingest 1-3mg/d.

Pregnancy

. Systemic absorption of adapalene across human skin is low, with none being detected in the plasma of 6 patients treated for acne in a standardized fashion for 5d with 2g. There are no adequate reports or well-controlled studies of adapalene in pregnant women. Women of child-bearing age should be fully informed of the risks and the importance of effective contraception. This also applies to patients with moderate forms of psoriasis, for which topical tazaroten is indicated.

Fetal Health

There are no adequate studies of adapalene in human pregnancy. It is unknown whether adapalene crosses the human placenta. Though the pharmacology is encouraging, there are several reports in humans associating adapalene with fetal malformation after cutaneous exposure. The available information is insufficient to conclude cause and effect. Oral administration to rodents at 100-200the MRHD increased the risk of malformation. No abnormalities were seen in pregnancies exposed to lower concentrations.

Breastfeeding

There is no published experience in nursing women. It is unknown whether adapalene enters human breast milk. Considering the dose and route, it is unlikely to pose a significant risk to the Breastfeeding neonate.

Pregnancy

. An endogenous purine-based nucleoside, IV adenosine is the first choice for short-term management of paroxysmal supraventricular arrhythmia after a vagal maneuver fails. Co-administration of midazolam safely reduces recall of the unpleasant effects of adenosine. For long-term therapy, b- blocking agents with b1selectivity are first-line drugs; class Ic agents and the class III drug sotalol are effective therapeutic alternatives. Adenosine has been used on multiple occasions during

Pregnancy

to treat paroxysmal SVT.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Adenosine crosses the human placenta, and though the kinetics remain to be detailed, it enhances placental perfusion. Rodent studies are reassuring, revealing no evidence of 13 teratogenicity. Adenosine has been administered successfully on a number of occasions directly into the umbilical vein to achieve control of a fetal SVT.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Adenosine is a normal constituent of human breast milk, though the short t/2 suggests little, if any, of the exogenously administered adenosine will enter the milk.

Pregnancy

. In some countries, albuterol has been used as a tocolytic agent given IV, SC, or PO (also see terbutaline or ritodrine, whose efficacy it compares to). There is no evidence it will stop preterm or term labor. The maximum delay (compared to placebo), though, of 48h should permit maternal administration of corticosteroids. b-Mimetic tocolysis is associated with pulmonary edema, especially with multiple gestation, or in women concurrently receiving glucocorticoid therapy to hasten fetal lung maturation, or in association with infection. The mechanism is unclear. Treatment consists of oxygen supplementation and diuresis. Maternal serum glucose and plasma insulin levels peak soon after cessation of therapy and return to preinfusion levels within 2-3h. The decline in potassium is gradual and plateaus after 2h. Once the albuterol 15 infusion is stopped, the potassium returns to normal by 2h. Total WBC counts increase within an hour of initiating therapy. There is no need to administer insulin for hyperglycemia and/or potassium for hypokalemia unless the patient is a known diabetic or is severely affected and requires immediate surgery.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Albuterol appears to cross the human placenta, though the kinetics remain to be elucidated. Less than 10% is absorbed when administered by inhalation. There is no convincing evidence of teratogenicity after 1st trimester exposure. In general, long-term follow-up studies of infants exposed to b-mimetic tocolysis are reassuring. Albuterol, like other b-adrenoceptor agonists, is associated with a reduction in the incidence of RDS. A single abstract suggests an increased risk of newborn retinopathy. Albuterol is teratogenic in mice at doses lower than those used in humans.

Breastfeeding

There is no published experience in nursing women. It is unknown whether albuterol enters human breast milk. Other b-adrenoceptor agonists such as ritodrine and terbutaline are considered safe for breastfeeding. Systemic absorption after inhalation is 10% or less.

Pregnancy

. There are no adequate reports or well-controlled studies of alendronate in pregnant women. There appears only one case report of its use during pregnancy; the woman did respond. Alendronate is superior to conjugated estrogens (with or without medroxyprogesterone) for the prevention of bone loss in elderly women, though the combination is superior.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Adult plasma levels are usually below the level of detection. There was no evidence of teratogenicity in two case series. Alendronate crosses the rodent placenta, decreasing bone density and delaying delivery. Both the total and ionized calcium are reduced in the rodent mother and fetus. The toxic effects are reversed by calcium administration. 17

Breastfeeding

There is no published experience in nursing women. It is unknown whether alendronate enters human breast milk. However, the risk to the breastfed neonate is likely low considering the low maternal systemic levels.

Pregnancy

. Alfentanil is a short-acting narcotic with rapid onset. As with other lipophilic opioids, alfentanil reduces the total dose of local anesthetic analgesic needed to provide comfort when combined with bupivacaine for epidural analgesia while diminishing the likelihood of an undesired motor blockade. IV alfentanil given just prior to intubation reduces the associated pressor response in women with preeclampsia.

Fetal Health

Alfentanil crosses the placenta when given IV, though its transfer rate is lower than fentanyl (which approximates antipyrine). Neither human embryo toxicity nor teratogenicity is reported, though 1st trimester human data are limited. Alfentanil is embryotoxic in rodents when given for 10-30d at doses 2-3the MRHD. One limited monkey study concluded offspring had impaired ability to do simple cognitive tasks at 2-3mo of age after exposure at 14w gestation. Lipophilic and hydrophilic characteristics of the drug influence placental transfer, as do fluctuations in maternal flow. Neonatal depression characterized by reduced active and passive tone is reported when alfentanil is given shortly before delivery. Occasionally, a narcotic antagonist is necessary. There are no reported fetal or neonatal effects after its use for conduction anesthesia.

Breastfeeding

Alfentanil is excreted into human the breast milk, though the amount excreted is too small to have any significant effect on the newborn.

Pregnancy

. There are no adequate reports or well-controlled studies of allopurinol in pregnant women. It is rarely indicated for its traditional indications in pregnant or lactating women. There is a single report of a woman treated during

Pregnancy

for primary gout with allopurinol. She delivered a healthy child at 35w. More often, allopurinol has been used during

Pregnancy

for women undergoing treatment of acute leukemia. Of future interest is its potential as an antioxidant. Allopurinol was used unsuccessfully in one trial for the treatment of established preeclampsia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Allopurinol readily crosses the ovine placenta, where it reaches equilibrium within 30min. It reduces superoxide 20 generation in the brains of fetuses subject to intermittent umbilical cord occlusion. There is no evidence that allopurinol is teratogenic in humans. Cleft palate and skeletal defects are reported in some rodents.

Breastfeeding

Allopurinol and its metabolite oxypurinol are excreted into breast milk to a limited degree and are considered compatible with breastfeeding. The average daily dose of allopurinol consumed by a 3kg neonate would be 0.6mg and of oxypurinol would be 24mg.

Pregnancy

. Migraine is a paroxysmal disorder with attacks of headache, N/V, photo- and phonophobia, and malaise. There is no published experience with almotriptan during pregnancy. Clinically, it is similar to sumatriptan, for which there is experience with during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether almotriptan crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically, though embryo lethality was observed at 1000the MRHD, and prolongation of

Pregnancy

at 160the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether almotriptan enters human breast milk.

Pregnancy

. Aloe vera gel comes from the inner tissue of the leaf and contains a myriad of compounds. Two FDA advisory panels concluded there was insufficient evidence that aloe vera is useful for the treatment of minor burns, cuts, or vaginal irritation. However, a recent study suggests aloe vera may accelerate wound healing by 22 promoting gap junctional intercellular communication and proliferation of human skin fibroblasts. There are no adequate reports or well-controlled studies in pregnant women. It should never be ingested during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses.

Breastfeeding

There is no published experience in pregnancy. However, considering the topical route, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. There are no published reports of alosetron use during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether alosetron crosses the human placenta. Rodent studies are generally reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically, with the exception of the mouse, where cleft palate and skeletal defects were reported.

Breastfeeding

There is no published experience in nursing women. It is unknown whether alosetron enters human breast milk. Alosetron is excreted into the milk of lactating rats.

Pregnancy

. Alprazolam is rarely indicated during pregnancy. There are few published reports of alprazolam use during pregnancy. Abrupt cessation of therapy is associated with a discontinuation-emergent 24 syndrome that includes neuropsychiatric, GI, dermatologic, CV, and visual symptoms.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. While there is no evidence that alprazolam is a human teratogen by either case reports or post-marketing surveillance, diazepam has been associated with fetal malformations. There is also concern based on studies with other benzodiazepines that postnatal behavior might be altered by antenatal exposure. Neonatal withdrawal has been reported. Treatment with phenobarbital is beneficial. In rodents, mice exposed to alprazolam demonstrate more individual than group activities and avoid open areas, and the males are more aggressive.

Breastfeeding

Alprazolam enters breast milk by passive diffusion, achieving an M:P ratio of 0.36 ingesting 0.3-5mcg/kg/d. This is approximately 3% of the weight-adjusted maternal dose. Though the risk is reasonably small, alprazolam should be avoided during lactation because of the potential that it might alter neurodevelopment and because of the documented risks of withdrawal.

Pregnancy

. There are no adequate reports or well-controlled studies of alteplase in pregnant women. There are case reports of its use during

Pregnancy

for the treatment of PE, MI, and peripheral thrombosis without an apparent increase in risk for hemorrhage, abruption, and PROM or preterm labor.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether alteplase crosses the human placenta. It could theoretically interfere with implantation. In light of its high molecular weight, alteplase is unlikely to cross the placenta. Rodent teratogenicity studies have not been conducted.

Breastfeeding

There is no published experience in nursing women. While tissue plasminogen activator is a normal constituent of human breast milk, it is unknown whether alteplase increases that level.

Pregnancy

. The published experience with amantadine during

Pregnancy

consists of isolated case reports. Amantadine has also been used to treat the fatigue associated with MS. There has been a progressive increase in amantadine resistant influenza A.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether amantadine crosses the human placenta. The human experience is of concern. 27 There are several case reports of CV abnormalities in exposed fetuses. Rats exposed to 7the MRHD show embryotoxicity and a variety of malformations, while there is no effect at doses 5-6the MRHD.

Breastfeeding

Amantadine is excreted in trace amounts into human milk. Though the kinetics and safety are unknown, the unsupplemented term infant would ingest <1mg/d assuming an M:P ratio of 1.

Pregnancy

. There are no adequate reports or well-controlled studies of ambenonium in pregnant women. The published experience consists of small series and case reports. Ambenonium is similar in action to neostigmine, but longer acting and with a lower incidence of GI Side effects include cardiac arrest, bronchospasm, cholinergic crisis, salivation, fasciculation, headache, drowsiness, and GI abnormalities such as diarrhea and abdominal pain. 28

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Ambenonium is not likely to cross the placenta because it is ionized at physiologic pH. However, other cholinesterase inhibitors have been associated with transient muscular weakness in the neonate. Breastfeeding There is no published experience in nursing women. Ambenonium is not likely to be excreted into breast milk because it is ionized at physiologic pH.

Pregnancy

. There are no adequate reports or well-controlled studies of amikacin in pregnant women.

Pregnancy

increases the maternal clearance of aminoglycosides in general. Women with normal renal function should receive a dose of amikacin that reflects the increased clearance.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Placental transfer of amikacin may be slightly higher than the b-lactams but is lower than maternal levels. 29 Aminoglycosides can damage the fetal kidney presumably because of delayed clearance, and irreversible failure has been reported after some aminoglycosides, but not amikacin. Amikacin may have less fetal renal toxicity than gentamicin. There is no evidence of teratogenicity or interference with fertility. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Amikacin is excreted into breast milk, but at low concentrations. Oral absorption is poor, suggesting little systemic risk to the neonate.

Pregnancy

. There are no adequate reports or well-controlled studies of amiloride in pregnant women. The published experience is limited to the occasional case report.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Amiloride crosses the placenta in modest amounts. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses 20-25higher than the MRHD.

Breastfeeding

Amiloride is concentrated in breast milk and should probably be avoided while breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of aminocaproic acid in pregnant women. It has been used in a variety of hemorrhagic circumstances. The literature consists predominantly of case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether aminocaproic acid crosses the human placenta. Aminocaproic acid decreases implantation in a variety of animal models. Rodent teratogenicity studies have not been reported.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether aminocaproic acid enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of aminoglutethimide in pregnant women. Aminoglutethimide may cause adrenocortical hypofunction, especially under stressful conditions. Patients should be treated with hydrocortisone (not dexamethasone) and a mineralocorticoid. Aminoglutethimide is also used to treat women with estrogen- sensitive breast cancer.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Pseudohermaphroditism is observed in about 2/5000 pregnancies treated with aminoglutethimide. Rodent studies revealed embryotoxicity and teratogenicity at doses smaller than those usually recommended for humans.

Breastfeeding

There is no published experience in nursing women. It is unknown whether aminoglutethimide enters human breast milk.

Pregnancy

. Aminophylline is a mixture of theophylline and theophylline base. Approximately1=3 of pregnant women with asthma get worse,1=3 get better, and1=3 remain clinically unchanged. Well-controlled asthma does not affect

Pregnancy

outcome; uncontrolled asthma may increase the risk of IUGR and preterm delivery. There are no adequate reports or well-controlled studies of aminophylline in pregnant women, but there is a long clinical experience. Clearance and the volume of distribution appear increased by pregnancy. IV aminophylline is not recommended unless the patient requires hospitalization. Even then, randomized trials suggest it provides no benefit over inhaled steroids. Uterine blood flow, as reflected by Doppler flow, is unaffected. Drug interactions are common and should be sought before prescribing.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Aminophylline crosses the human placenta rapidly, reaching an F:M ratio approaching unity. While there is no substantive evidence in humans, teratogenicity and embryotoxicity are reported in rats and rabbits at doses that exceed the MRHD by 20-50?. This effect is dose dependent. The proconvulsant effect of aminophylline on cortical epileptic after-discharges varies during ontogeny. Recently, it was suggested that the combination of maternal magnesium sulfate and aminophylline reduced the incidence of neonatal intracranial hemorrhage in preterm neonates. This observation remains to be confirmed.

Breastfeeding

Aminophylline is excreted into breast milk and may cause irritability or other signs of toxicity in nursing neonates. However, it is generally considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of amiodarone in pregnant women. The published experience is limited to fewer than 100 pregnancies. There are many alternatives to amiodarone during pregnancy. 35

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Placental transport occurs, but studies suggest low transfer especially when the umbilical venous pressure is elevated. Amiodarone has been used in isolated instances to treat a fetal arrhythmia. Among 64 pregnancies exposed to amiodarone, 17% of neonates had hypothyroidism (10 detected at birth, 1 in utero), 18% of whom had a goiter. Hypothyroidism was transient in all, though 5 were treated short-term. Neurodevelopmental assessment of the hypothyroid infants, when carried out, revealed in some instances mild abnormalities often similar to the nonverbal learning disability syndrome. These features were also reported in some amiodarone-exposed euthyroid infants, suggesting a direct neurotoxic effect of amiodarone during fetal life. Fetal hypothyroidism has been reported in amiodarone- resistant fetal arrhythmia.

Breastfeeding

Amiodarone is excreted in breast milk at concentrations high enough to have a pharmacologic effect. The reported M:P ratio ranges from 4.6 to 13, with concentrations in women ingesting 400mg/d ranging from 2.8 to 16.4mg/L. Neonatal hypothyroidism is reported.

Pregnancy

. Depression is common during and after pregnancy, but typically goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. Despite the fact that pregnant women are often exposed to tricyclic agents, there are no well-controlled studies of amitriptyline during pregnancy. The drug is metabolized by CYP2D6, which is reduced in some Caucasians (about 7-10% of Caucasians are so-called poor metabolizers); the prevalences of poor metabolizers among Asian, black, and other populations are unclear. Poor metabolizers have higher than expected plasma concentrations when given usual doses. Thus, serum levels should be monitored during pregnancy. Although amitriptyline has no effect on placental blood flow in gravid sheep, the pressor response to NE, but not phenylephrine, is enhanced. Off-label uses include bulimia, nocturnal enuresis, panic migraine, panic disorder, and postherpetic neuralgia.

Fetal Health

Both amitriptyline and its sib, nortriptyline, cross the human placenta. Though there is no causal evidence, case reports suggest CNS/limb abnormalities and developmental delay. While rodent studies are generally reassuring at doses below 10the MRHD, studies at 10-33the MRHD reveal CNS and facial abnormalities. Long-term effects on serotonergic receptors are postulated but not confirmed.

Breastfeeding

Multiple studies reveal that, while amitriptyline is excreted into the breast milk, the neonatal concentrations are extremely low.

Pregnancy

. There are no well-controlled studies in women of amlodipine during pregnancy. Other calcium channel antagonists are used as inhibitors of myometrial contraction, and amlodipine has similar properties. There are no reports of its use as a tocolytic agent.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether amlodipine crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses 8- 23the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether amlodipine enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of amobarbital in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Amobarbital crosses the human placenta, achieving an F:M ratio near unity. Though there was some suggestion of a nonspecific risk of malformation in exposed offspring, subsequent studies were reassuring.

Breastfeeding

There is no published experience in nursing women. It is unknown whether amobarbital enters human breast milk, though similar agents do.

Pregnancy

. Depression is common during and after pregnancy, but typically goes unrecognized.

Pregnancy

is not a reason a priori to discontinue psychotropic drugs. There are no adequate reports or well-controlled studies of amoxapine use in pregnant women. There are only scattered case reports to draw upon. Amoxapine is similar in efficacy to imipramine.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Rodent studies are generally reassuring, revealing no evidence of teratogenicity. Embryotoxicity was seen at human dose levels, and fetotoxicity at multiples of the MRHD.

Breastfeeding

Amoxapine is excreted in the breast milk, though the levels were <180mcg/L (<20mcg/kg/d) in one study after 250mg/kg/d, representing <20% of the maternal plasma level.

Pregnancy

. Similar to ampicillin, amoxicillin is generally considered safe during pregnancy. It provides a >90% cure rate for Chlamydia, and is the most cost-effective treatment followed by a single 1g dose of azithromycin for nonresponders.

Fetal Health

Amoxicillin crosses the placenta and may reach therapeutic levels in the fetus and AF after maternal administration. It is generally considered safe for the fetus. There are no reports of associated defects, and rodent studies are reassuring.

Breastfeeding

Amoxicillin is excreted into the breast milk in low concentrations, but is generally considered safe during lactation.

Pregnancy

. Oral amoxicillin is poorly absorbed during labor. Amoxicillin- clavulanate does not improve treatment of preterm labor and intact membranes. While amoxicillin-clavulanate is associated with prolongation of the latency interval after PPROM, there is a greater risk of necrotizing enterocolitis compared to either placebo or erythromycin. Thus, erythromycin is preferred for this indication. The incidence of maternal infectious complications is reduced by most antibiotic regimens. More recently, amoxicillin-clavulanate has been used as part of a 44 multidrug regimen to treat drug-resistant tuberculosis during pregnancy. (See amoxicillin.)

Fetal Health

Amoxicillin-clavulanate is unassociated with malformation in animal and human studies. However, the numbers of human studies are limited. Amoxicillin-clavulanate use may increase the risk of necrotizing enterocolitis when used for prophylaxis in women with PPROM. (See amoxicillin.)

Breastfeeding

This class of drug is excreted in milk, but no adverse effects are reported.

Pregnancy

. Amphetamines are noncatecholamine sympathomimetic amines with both peripheral and CNS activities. There are no adequate reports or well-controlled studies of amphetamine- dextroamphetamine in pregnant women. Methamphetamine is metabolized to amphetamine. Amphetamine dependency is associated with preterm delivery. With perhaps the exception of narcolepsy, amphetamines should rarely be used during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Infants born to amphetamine-dependent women show signs of withdrawal, suggesting placental transfer. Amphetamine is associated with an increased prevalence of IUGR. It is embryotoxic and teratogenic in some rodents when given at high doses. Case-control studies do not reveal a pattern of teratogenicity, though scattered case reports list various defects associated with 1st trimester usage. Antenatal amphetamine exposure is associated with aggressive behavior and delayed development in children under 14y of age.

Breastfeeding

Amphetamine is concentrated in human breast milk and generally considered incompatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of amphotericin in pregnant women. It remains the drug of choice for systemic, invasive mycotic infections, whether life-threatening or less severe. Amphotericin has been used extensively during

Pregnancy

without increased risk of complications. Unfortunately little if any information is available regarding the safety of the newer lipid formulations. It has also been used for the treatment of meningoencephalitis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Amphotericin crosses the human placenta and is deposited in the fetal tissues. Therapeutic levels are found in fetal tissues weeks after cessation. There are no reports of teratogenicity. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether amphotericin enters human breast milk.

Pregnancy

. Well absorbed orally except during labor, ampicillin is one of the most commonly used antibiotics during pregnancy. In addition to the noted indications, ampicillin was used without success in combination with tocolytic agents to delay or avoid preterm delivery. In comparison to nonpregnant women,

Pregnancy

significantly increases the ampicillin elimination rate constant and total body clearance and decreases the serum t/2 and AUC. As a result, the dose during

Pregnancy

should be increased and the interval decreased. Ampicillin clearance is reduced by pyelonephritis and rises with successful treatment. This suggests the dosing interval should be reduced from 6h to 4h after the first 24h of therapy. When combined with sulbactam, ampicillin significantly prolongs the latency interval between rupture and delivery. Ampicillin alone is less effective.

Fetal Health

There is a wide body of clinical experience with ampicillin during pregnancy. There is no evidence of teratogenicity in either humans or rodents. Throughout pregnancy, fetal drug levels reach maternal equilibrium 1-3h after administration; thereafter, fetal drug levels exceed maternal values. AF levels are low during early pregnancy, but rise with advancing gestation and may exceed maternal values 6-8h after drug administration.

Breastfeeding

Minimal amounts of ampicillin are excreted in breast milk. It is generally considered compatible with breastfeeding.

Pregnancy

. Ampicillin-sulbactam is a reasonable selection for prophylaxis in women undergoing cesarean section. Ampicillin does not prolong the latency interval after PPROM unless paired with sulbactam. In comparison to nonpregnant women,

Pregnancy

significantly increases the ampicillin elimination rate constant and total body clearance and decreases the serum t/2 and AUC. As a result, the dose during

Pregnancy

should be increased and the interval decreased. Ampicillin clearance is reduced by pyelonephritis and rises with successful treatment. This suggests the dosing interval should be reduced from 6h to 4h after the first 24h of therapy.

Fetal Health

Ampicillin-sulbactam reduces neonatal infectious morbidity after PPROM, but to no greater extent than erythromycin, which also prolongs the latency interval. There is no substantive evidence of teratogenicity. Rodent studies are reassuring, revealing no 50 evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Minimal amounts of ampicillin-sulbactam are excreted in breast milk. It is generally considered compatible with breastfeeding.

Pregnancy

. There are limited published case reports of amprenavir use during pregnancy.

Fetal Health

Amprenavir crosses the human placenta. In one study, umbilical cord blood concentrations were below detection in 10/40 samples for nelfinavir and 25/40 samples for its metabolite M8, 9/11 samples for ritonavir, 4/6 samples for indinavir, and 5/6 samples for saquinavir, but concentrations were detectable in 3/3 samples 51 for amprenavir. In various rodents, doses of amprenavir well below the MRHD were associated with an increased abortion rate and deficient long bone ossification.

Breastfeeding

It is unknown whether amprenavir is excreted in human breast milk. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. Pregnant women with essential thrombocythemia have an increased risk of 1st trimester loss that is not predictable by the pre

Pregnancy

platelet count or reducible by aspirin therapy. There are no adequate reports or well-controlled studies of anagrelide in pregnant women. There are only scattered case reports of its use during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Rodent studies are reassuring, revealing no evidence of teratogenicity. However, very high doses were associated with delayed delivery and its sequelae.

Breastfeeding

There is no published experience in nursing women. It is unknown whether anagrelide enters human breast milk.

Pregnancy

. There are no published reports of anakinra use during pregnancy. Native IL-1 type 1 receptor antagonist has variably been associated with recurrent

Pregnancy

loss, and is increased in AF and umbilical venous blood obtained from pregnancies complicated by PPROM.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether anakinra crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether anakinra enters human breast milk. Native IL-1 type 1 receptor antagonist is present in breast milk, and the concentration is increased by mastitis.

Pregnancy

. Psoriasis is a chronically recurring inflammatory disease that affects the skin, scalp, and joints.

Pregnancy

may precipitate pustular psoriasis. There are no adequate reports or well-controlled studies of anthralin in pregnant women. Though it is generally considered safe for use during pregnancy, there are few data to support a conclusion either way. 54

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Rodent teratogenicity studies have apparently not been conducted.

Breastfeeding

There is no published experience in nursing women. It is unknown whether anthralin enters human breast milk. The route and dosing frequency suggest it is unlikely the Breastfeeding neonate would ingest a clinically relevant amount.

Pregnancy

. Not surprisingly, there are no adequate reports or well-controlled studies of antihemophilic factor in pregnant women since the factor VIII deficiency is X-linked. Unbalanced lyonization or crossover during meiosis would account for the rare reports in women if accurate. Replacement is of little clinical use in women with an acquired inhibitor of factor VIII.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Animal studies have not been performed, explaining the FDA classification as C.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women.

Pregnancy

. There are no adequate studies of antithrombin III concentrate in pregnant women. ATIII consumption during normal

Pregnancy

is increased to the level associated with sepsis in the nonpregnant patient. Women with congenital ATIII deficiency have dramatically increased risk of thromboembolic disease during pregnancy. Heparin may be ineffective, depending upon the ATIII level. Replacement is effective prophylaxis and treatment of acute thrombosis and must be performed on an ongoing basis. Preeclampsia is a cause of acquired ATIII deficiency secondary to 56 increased consumption. Several studies suggest ATIII replacement may improve maternal outcome in women with preeclampsia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. There are no reports of adverse fetal effects, and the size of the molecule indicates placental transfer is unlikely. Rodent teratogenicity studies apparently have not been conducted. As an endogenous substance, antithrombin III concentrate is unlikely to have any adverse fetal effects.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether antithrombin III concentrate enters human breast milk.

Pregnancy

. There are no reports of arbutamine use during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Rodent studies are reassuring, revealing no evidence of teratogenicity. 57

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether arbutamine enters human breast milk. However, considering the indication, it is unlikely the breastfed neonate would ingest clinically relevant amounts after one-time use.

Pregnancy

. There is no published experience with ardeparin during pregnancy. This class of drugs is being used with increasing frequency during

Pregnancy

for the treatment of thrombophilia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Its molecular weight suggests ardeparin does not cross the placenta. Rodent studies at up to 3the MRHD revealed no evidence of impaired fertility or fetal harm. However, when administered at 7and 11the MRHD, scoliosis and cardiac defects, respectively, were noted.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether ardeparin enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of argatroban in pregnant women. The published experience is limited to case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether argatroban crosses the human placenta. Rodent studies have not revealed evidence of either impaired fertility or teratogenicity, though the doses used were smaller than those employed clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether argatroban enters human breast milk. Argatroban is detected in rat breast milk.

Pregnancy

. Ascorbic acid is an essential vitamin that acts as a coenzyme for collagen formation, tissue repair, and the synthesis of lipids and proteins. It has both reducing and antioxidant properties and is necessary for many physiologic functions (e.g., metabolism of iron and folic acid, resistance to infection, and preservation of blood vessel integrity). Signs and symptoms of early ascorbic acid deficiency include malaise, irritability, arthralgia, hyperkeratosis, nosebleed, and petechial hemorrhages. Prolonged deficiency leads to clinical scurvy. There has been limited study of ascorbic acid during human pregnancy. Supplementation with ascorbic acid and vitamin E does not reduce the rate of preeclampsia in women at high risk. Women with established early-onset preeclampsia (<32w) likewise do not benefit from pharmacologic doses. Ascorbic acid is consumed during labor, perhaps because of oxygen free radical generation during the ischemia-reperfusion associated with uterine contractions. Women who consume low amounts of ascorbic acid appear to have an increased risk of developing gestational diabetes. However, maternal supplementation of replete women with 500mg daily does not seem to alter the serum level after 1mo. Supplementation does not reduce the prevalence of preterm delivery.

Fetal Health

There are no adequate and well-controlled studies in human fetuses. It is unknown how ascorbic acid crosses the human placenta. In the pig, transfer increases with advancing gestational age. In the human, umbilical vein ascorbic acid levels are lower 60 in the preterm compared to the term fetus. Ascorbic acid concentrations in cesarean and vaginal delivery patients are higher in AF than fetal plasma. In one randomized trial initiated at 35w gestation, maternal intake of 500mg ascorbic acid failed to alter the fetal serum level from placebo. High doses of ascorbic acid taken during

Pregnancy

are reported to cause scurvy in infants removed from this environment at birth. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. In diabetic rats, ascorbic acid supplementation reduces the malformation rate.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Ascorbic acid is excreted in breast milk; the RDA for Breastfeeding women is 90-100mg. The milk concentration corresponds with maternal dietary intake, but excessive supplementation has little incremental effect on it. The level in refrigerated milk declines by a third within 24h.

Pregnancy

. Aspirin is a potent drug with a complex and still incompletely understood mechanisms of action. It is ubiquitous in the pharmacopeia, being combined with a multitude of agents. Aspirin is recommended by the American Heart Association for women with a 10y risk of coronary heart disease of 10% or 62 higher, and by the U.S. Preventive Services Task Force for women whose 5y risk of coronary heart disease is 3% or higher. Women ingesting large quantities of aspirin are at risk for myriad complications. Though one prospective case-control study suggested that the antenatal use of ibuprofen, naproxen, and possibly aspirin but not acetaminophen increased the risk of spontaneous abortion; the risk for aspirin was not confirmed in a more recent study. Chronically high salicylate levels are associated with prolonged pregnancy, increased puerperal bleeding, decreased birth weight, and stillbirth. It is generally recommended that high doses of aspirin be avoided during the last trimester. Low-dose aspirin plus heparin appears effective treatment for antiphospholipid syndrome characterized by recurrent 1st trimester losses. It is not an effective treatment for idiopathic recurrent losses absent a thrombophilia. Aspirin and moderate- intensity warfarin appear equally effective for preventing recurrent stroke for women with a single positive antiphospholipid antibody test result and prior stroke. Controversy continues regarding the benefit of low-dose aspirin for the prevention of preeclampsia, though no complications of treatment have been documented and several meta-analyses suggest a modest reduction in preeclampsia and IUGR. In one randomized controlled trial, almost 20,000 women underwent uterine artery Doppler screening at 22-24w; 560 women with abnormal Doppler flow profiles were randomized to low-dose aspirin (150mg/d) or placebo. There was no improvement in either maternal or perinatal outcome.

Fetal Health

Aspirin does cross the placenta. Maternal aspirin ingestion has been linked to gastroschisis and small intestine atresia independent of fever or cold symptoms. Low-dose aspirin doses alter fetal cyclooxygenase activity, but no sequelae are known.

Breastfeeding

The use of aspirin in single doses should not pose any risk to the Breastfeeding newborn. In contrast, women on high doses of aspirin such as that for arthritis or rheumatic fever might best avoid breastfeeding, as the neonatal salicylate level may reach therapeutic levels.

Pregnancy

. Hypertension complicates 5-10% of pregnancies and is a leading cause of maternal and perinatal death and morbidity. Severe hypertension (systolic BP = 170mmHg and/or diastolic BP = 110mmHg) should be treated immediately. Mild, chronic hypertension is associated with increased maternal and fetal risks, but there is no consensus as to whether mild to moderate hypertension should be treated during pregnancy. The incidence of transient severe hypertension, antenatal hospitalization, proteinuria, and neonatal RDS may be decreased by therapy, but fetal growth may be impaired. In one small trial, atenolol reduced the incidence of preeclampsia in women selected for increased cardiac output. Of all b-blockers, the evidence that atenolol is associated with IUGR is the strongest, but appears to reflects excess maternal b-blockade, causing a decrease in cardiac output. Atenolol has also been used to treat congenital long QT syndrome during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Atenolol crosses the placenta. There is no substantive evidence of teratogenicity. As a group, b-blockers are associated with IUGR, though controversy continues as to whether this is drug or disease related. Atenolol reduces cardiac output, and failure to reduce the dose to prevent an excessive decline in output is associated with IUGR. Some rodent studies reveal a dose-dependent increase in embryo/fetal resorption.

Breastfeeding

Atenolol is concentrated in breast milk, and significant bradycardia may occur in newborns nursed by women on atenolol. It should probably be avoided.

Pregnancy

. Compared to fluvastatin, lovastatin, pravastatin, or simvastatin, atorvastatin is associated with the lowest level of resource use and costs when used to treat patients with hypercholesterolemia. Atorvastatin is also associated with the highest percentage of patients achieving their desired clinical targets. There is a single case report of atorvastatin use during

Pregnancy

after inadvertent exposure. Though the outcome was normal, the safety of atorvastatin during

Pregnancy

remains to be established.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Atorvastatin is an inhibitor of P-glycoprotein. While it is unknown whether atorvastatin crosses the human placenta, it crosses the rodent placenta. One review of 214

Pregnancy

exposures and 70 informative cases noted 31 adverse outcomes in 66 22 neonates with structural defects, 4 with IUGR, and 5 fetal deaths. There were two principal groups of recurrent structural defects: cerivastatin and lovastatin were associated with 4 reports of severe, midline CNS defects; simvastatin, lovastatin, and atorvastatin were all associated with limb deficiencies, including 2 similar complex lower limb defects after simvastatin exposure. There were also 2 cases of VACTERL among the limb deficiency cases. All adverse outcomes were reported following exposure to cerivastatin, simvastatin, lovastatin, or atorvastatin, which are lipophilic and should equilibrate between maternal and fetal compartments. None were reported after exposure to pravastatin, which is poorly transported across the rodent placenta. These authors suggest that statins may have secondary effects on sterol- dependent morphogens such as Sonic Hedgehog. Further study is necessary. Atorvastatin reaches fetal hepatic concentrations similar to maternal plasma. While there is no evidence of teratogenicity in rodents even at high doses, there is a dose-dependent increase in IUGR, a decrease in survival, and behavioral abnormalities that were gender-dependent. Rare structural defects have occasionally been reported in association with other HMG-CoA reductase inhibitors.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether atorvastatin enters human breast milk. However, its poor oral absorption and high degree of protein binding suggest it is unlikely clinically relevant amounts will be found. Atorvastatin is excreted into the breast milk of rats.

Pregnancy

. There are no adequate reports or well-controlled studies of atovaquone during pregnancy. Several studies suggest the combination of atovaquone and proguanil is effective malaria prophylaxis. The pharmacokinetics of atovaquone were recently determined in women with multidrug-resistant falciparum malaria treated by artesunate-atovaquone-proguanil during their 2nd and 3rd trimesters. The triple combination was well- tolerated and highly effective. The outcomes of

Pregnancy

were all normal. Population mean (?SEM) oral clearance (Cl/F) estimates were 313 ? 33ml/h/kg and 1109 ? 43ml/h/kg, total apparent volume of distribution (Vd/F) was 13.0 ? 1.3l/kg and 22.9 ? 1.4l/kg, and terminal elimination t/2 was 29.1h and 14.3h for atovaquone and proguanil, respectively. Using conventional and population analyses, Cl/F and Vd/F estimates for atovaquone and proguanil were 2and plasma concentrations <1=2 those reported in healthy subjects and patients with acute malaria. This suggests the dose of atovaquone and proguanil should be increased for the treatment of malaria during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Published studies do not permit any conclusion on safety. It is unknown whether atovaquone crosses the human placenta. Atovaquone crosses the rodent placenta, reaching an F:M ratio approximating 0.3. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Though maternal and placental parasitemia is reduced by maternal pharmacotherapy, there is as yet no detectable reduction in perinatal mortality.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether atovaquone enters human breast milk. In rats, the M:P ratio approximates 1:3.

Pregnancy

. This is a fixed combination agent. Falciparum malaria has a higher risk of morbidity and mortality during pregnancy. There are no adequate reports or well-controlled studies of atovaquone- proguanil in pregnant women. At full term, both oral clearance (Cl/F) and the total apparent volume of distribution (Vd/F) estimates for both drugs were roughly 2and plasma concentrations1=2 that reported in healthy nonpregnant patients and those with acute malaria. Proguanil biotransformation into active antimalarial metabolites may be impaired during late pregnancy. These findings suggest the dosing regimen may need 69 to be increased during

Pregnancy

to ensure efficacy and minimize the risk of resistance. (See comments under atovaquone.)

Fetal Health

There are no adequate and well-controlled studies in human fetuses. It is unknown whether atovaquone-proguanil crosses the human placenta. The clinical experience is reassuring. Atovaquone crosses the rodent placenta, reaching an F:M ratio approximating 0.3. Rodent studies of atovaquone are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Rodent studies for proguanil too are reassuring, revealing no evidence of teratogenicity or IUGR, but the doses used have been insufficient to provide confidence in the conclusion. Though maternal and placental parasitemia is reduced by maternal pharmacotherapy, there is as yet no detectable reduction in perinatal mortality.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether atovaquone enters human breast milk. It is excreted into rodent milk, achieving an M:P ratio of about one third. Trace amounts of proguanil are found in human breast milk. Perhaps in response to the inadequate study, the CDC recommends that Breastfeeding women with infants <11kg should use mefloquine for malaria prophylaxis.

Pregnancy

. Atracurium is an intermediate-duration curare derivative producing effective surgical paralysis. There are no adequate reports or well-controlled studies of atracurium in pregnant women. The clearance and clinical duration of atracurium are unaltered during pregnancy. In contrast, the clearance of pancuronium is increased 27% during cesarean section, and the mean onset time and clinical duration of cisatracurium are significantly reduced.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Atracurium has been used in lieu of pancuronium to facilitate fetal procedures. While small amounts are shown to cross the human placenta, its use during cesarean section is not associated with neonatal sequelae. In theory, fetal toxicity could be a risk if used for long-term paralysis of a critically ill pregnant woman.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether atracurium enters human breast milk. Considering its application, atracurium is unlikely to affect the Breastfeeding newborn. While some rodent studies report an increase in malformations, they are confounded by the profound respiratory depression associated with the drug.

Pregnancy

. There are no adequate reports or well-controlled studies of atropine in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Atropine rapidly crosses the human placenta, and the fetus will respond to the direct administration of atropine.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether atropine enters human breast milk. 72

Pregnancy

. There are no adequate reports or well-controlled studies of attapulgite in pregnant women. Attapulgite was formerly part of the Kaopectate formulation, but was removed in 2003.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether attapulgite crosses the human placenta.

Breastfeeding

There is no published experience in nursing women. It is unknown whether attapulgite will alter breast milk.

Pregnancy

. There is no published experience with auranofin during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether auranofin crosses the human placenta. Rodent studies reveal an increased risk of embryo and fetal toxicity, gastroschisis, and umbilical hernia.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether auranofin enters human breast milk. Gold is excreted into rodent milk.

Pregnancy

. Azatadine is an antihistamine with antiserotonergic, anticholinergic, and sedative effects. There is no published experience during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies of azatadine in human fetuses. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether azatadine enters human breast milk.

Pregnancy

. Azathioprine is metabolized to 6-mercaptopurine. There are no adequate reports or well-controlled studies of azathioprine in pregnant women. Immune-related disorders are fairly common in reproductive-age women. Women with quiescent inflammatory bowel disease are likely to have an uncomplicated pregnancy, whereas women with active disease are more likely to have complications such as spontaneous abortions, miscarriages, stillbirths, and exacerbation of the disease. Most pregnancies treated with azathioprine end successfully, even in transplant patients. It has been used successfully for the treatment of autoimmune hepatitis during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Azathioprine crosses the human placenta; though the kinetics are unclear, it appears to reach equilibrium. The limited human experience (approximately 6 studies) is reassuring, and the drug should not be withheld if medically indicated. While no clear pattern of malformation is detectable in the large number of pregnant women exposed, isolated skeletal defects are reported. All immunosuppressants cross the placenta, and their long-term impact on the child later in life is unknown. There are also reports in neonates of reduced IgG and IgM, and leukopenia. It is unclear whether the reported increase in IUGR reflects disease or drug. Heightened immune responses were reported during the

Pregnancy

of a woman whose mother had been treated with azathioprine throughout pregnancy. Azathioprine is teratogenic in rodents treated with human-equivalent doses, producing a constellation of malformations that are both skeletal and visceral.

Breastfeeding

Azathioprine is excreted into breast milk, but the pharmacokinetics remain to be elucidated. In two women taking 75mg a day, the milk 6-mercaptopurine was <20mcg/L, suggesting the breastfed neonate would ingest <0.5% of the maternal dose. There are no well- documented instances of neonatal effect.

Pregnancy

. Azithromycin has a short serum t/2 in term pregnant women. Prolonged t/2 and high tissue levels occur in myometrium, placenta, and adipose tissue. When combined with doxycycline, it reduces the risk of postcesarean endomyometritis. Interconceptional use of azithromycin plus metronidazole does not reduce the prevalence of preterm birth compared to placebo. Considering its efficacy against other STDs and convenient dosing regimen, azithromycin is probably the treatment of choice for Chlamydia. Single-dose azithromycin may be as effective as penicillin G for the treatment of early syphilis. Partner pharmacotherapy is cost-effective. Azithromycin has been used in combination with artesunate as malaria prophylaxis. It was ineffective treatment to reduce lower genital tract colonization with Ureaplasma urealyticum in women with preterm labor. 77 Azithromycin also improves pulmonary function in women with cystic fibrosis and in women who are chronically infected with Pseudomonas aeruginosa.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Less than 3% of maternally administered azithromycin crosses the placenta. Not surprisingly, there have been no adverse effects reported in humans. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Azithromycin is excreted in breast milk in a dose-dependent fashion that would approximate 0.4mg/kg/d, a subclinical amount. No neonatal effects have been reported.

Pregnancy

. There are no adequate reports or well-controlled studies of aztreonam in pregnant women. It is one of many antibiotics of potential use during pregnancy. Aztreonam is as effective as gentamicin plus clindamycin for the treatment of puerperal endomyometritis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Aztreonam crosses the human placenta in therapeutic concentrations, suggesting it might be useful for antepartal chorioamnionitis. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in human fetuses. It is excreted into the breast milk at trace levels.

Pregnancy

. There is no published experience during pregnancy. Bacitracin enhances wound healing in nonpregnant surgical patients and reduces scarring compared to placebo.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether bacitracin crosses the human placenta. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level. Rodent teratogenicity studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether bacitracin enters human breast milk. However, considering the dose and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. There are no adequate reports or well-controlled studies of baclofen in pregnant women. The published experience is mostly limited to case reports, mostly of intrathecal use in women with MS. For example, one documents successful intrathecal use for the treatment of severe tetanus, and another the long-term treatment of severe spasticity after a C5 fracture. Baclofen proved superior to placebo for the relief of abortal pain.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether baclofen crosses the human placenta. There is a single case report of neonatal convulsions at 7d of age. Rodent studies reveal an increased prevalence of omphalocele, incomplete ossification of the sternum, vertebral arch widening, and neural tube defects when given at 10the MRHD.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Baclofen reduces sucking-induced prolactin release, but milk ejection is unchanged. Only about 0.1% of the maternal dose is excreted into human breast milk.

Pregnancy

. Balsalazide is a prodrug enzymatically cleaved in the colon to produce melsalamine. Though considered safe to use by some clinicians, there are no adequate reports or well-controlled studies of balsalazide in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether balsalazide crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether balsalazide enters human breast milk.

Pregnancy

. There are only case reports of basiliximab use during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether basiliximab crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether basiliximab enters human breast milk. However, considering the indication and dosing, one-time basiliximab use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. Asthma is associated with several complications during pregnancy. Inhaled corticosteroids are generally be considered the prophylactic medication of choice in pregnant women with persistent asthma, unless well controlled by either cromolyn or nedocromil. Beclomethasone effectiveness requires regular use. A recent randomized trial compared beclomethasone to oral theophylline for the treatment of moderate asthma. Thus, beclomethasone is considered a first-line agent along with budesonide during pregnancy.

Fetal Health

There are no well-controlled studies of beclomethasone in human fetuses. It is unknown whether beclomethasone specifically crosses the human placenta. Hypoadrenalism may occur in newborns of women using beclomethasone, suggesting placental transfer. Rodent studies using up to 10the MRHD revealed increased frequencies of fetal resorption, cleft palate, delayed ossification, agnathia, and embryocidal effect.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether beclomethasone enters human breast milk. Other steroids are excreted in low amounts.

Pregnancy

. There are no well-controlled studies of belladonna in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Belladonna rapidly crosses the placenta, producing a pharmacologic fetal vagotomy with subsequent tachycardia. It decreases fetal breathing. However, no adverse acute or chronic fetal effects are documented in women taking atropine. No association with malformations has been documented.

Breastfeeding

No adequate well-controlled studies determined the passage of belladonna in the breast milk; it is generally considered safe for breastfeeding.

Pregnancy

. The published experience during

Pregnancy

consists of case reports. However, this class of agents is associated with severe fetal renal toxicity. Once thought relatively safe in the 1st trimester, benazepril is now considered contraindicated throughout gestation.

Fetal Health

Benazepril may cause embryonic, fetal, and neonatal morbidity and death. ACEIs during the 2nd and 3rd trimesters of

Pregnancy

are associated with hypotension, neonatal skull hypoplasia, renal failure, and oligohydramnios. It is not known whether all ACEIs have the exact risks. Benazepril has in humans been associated with oligohydramnios that was reversible with discontinuation. Limited placental transfer is noted in the rat.

Breastfeeding

There is no published experience in nursing women. Minimal amounts of benazepril enter the breast milk.

Pregnancy

. There is no published experience with bendroflumethiazide during pregnancy. Thiazide diuretics should be avoided during

Pregnancy

except for the treatment of congestive heart disease. It has been suggested but not shown that diuretics in general may hinder placental perfusion by preventing normal plasma expansion. Thiazide diuretics are diabetogenic in some women. There are several reports of severe electrolyte imbalance in both mothers and newborns. Hemorrhagic pancreatitis has also been reported after thiazide exposure.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether bendroflumethiazide crosses the human placenta. Other thiazide agents readily cross. Fetal bradycardia associated with fetal hypokalemia has also been reported after maternal thiazide use. Though not associated with congenital defects, neonatal thrombocytopenia and hypoglycemia are reported. 87

Breastfeeding

There is no published experience in nursing women. Many thiazide diuretics are excreted into breast milk, but in low concentrations. They are generally considered safe for Breastfeeding women.

Pregnancy

. There are no well-controlled studies of benzocaine during pregnancy. It provides relief from perineal pain associated with episiotomy, especially when associated with a corticosteroid. Some practitioners use it as an alternative to lidocaine for the symptomatic relief of perineal herpetic lesions.

Fetal Health

There are no well-controlled studies of benzocaine in human fetuses. It is unknown whether benzocaine crosses the human placenta. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level.

Breastfeeding

There is no published experience in nursing women. However, considering the dose and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. Benzoyl peroxide is for external use only. It has been used for the treatment of acne since the 1930s. There are no well-controlled studies in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether benzoyl peroxide crosses the human placenta. Rodent teratogen studies have apparently not been conducted. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level.

Breastfeeding

There is no published experience in nursing women. It is unknown whether benzoyl peroxide enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of benztropine in pregnant women. The published experience is limited to isolated case reports.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether benztropine crosses the human placenta. Exposure to benztropine during the 1st trimester might be associated with CV defects. Neonatal paralytic ileus has been reported after benztropine use.

Breastfeeding

There is no published experience in nursing women. It is unknown whether benztropine enters human breast milk. No adverse neonatal effects are reported with other parasympatholytics such as atropine.

Pregnancy

. There is no published experience with bepridil during human pregnancy.

Fetal Health

There are no well-controlled studies during pregnancy. Decreased fetal weight and survival were reported in animals exposed to doses more than 30the MRHD. No teratogenic effects were noted in laboratory animals at the same dosages.

Breastfeeding

There is no published experience in nursing women. Bepridil is excreted into human breast milk, achieving an M:P ratio approximating 0.33 according to the manufacturer, but the kinetics remain to be clarified. Caution is indicated considering the long t/2 and high oral absorption.

Pregnancy

. b-Carotene is an antioxidant, and consuming foods rich in b-carotene may help protect from free radical damage. Some studies suggest dietary intake of b-carotene may reduce the risk of heart disease and cancer. There are no adequate reports or well-controlled studies in pregnant women. It has been suggested that millions of pregnant women annually suffer night blindness because of a deficiency. The safety of doses exceeding 6000 USP units during

Pregnancy

is not established.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. High doses of b-carotene are teratogenic (bone, heart). There is no evidence of teratogenicity in women consuming 8000-25,000IU per day. However, low levels in rodents is associated with a reduction in the number of nephrons.

Breastfeeding

There is no published experience in nursing women. b-Carotene enters human breast milk and raises its vitamin A level.

Pregnancy

. Betamethasone may increase the risk of maternal infection in women with PPROM, though most large studies reveal no increase. It can transiently cause an abnormal glucose tolerance test, will worsen existing diabetes mellitus, and is associated with pulmonary edema especially when given with a tocolytic agent in the setting of an underlying infection.

Fetal Health

Betamethasone crosses the human placenta and is one of the few drugs proven to improve perinatal outcome. Some of the beneficial effect on the lung may be lost if delivery occurs more than 14d after administration. Two courses more than a week apart significantly reduces perinatal morbidity following preterm birth. Outcomes at 2-3y of age after multiple courses are reassuring. About half of the drug is metabolized to inactive 11- ketosteroid derivatives. An increased risk of neonatal sepsis was suggested but not confirmed. Multiple courses of betamethasone are not recommended. Adverse effects noted in animal and human studies are magnified by repeated courses of steroids. They include a profound suppression of fetal breathing and movement, impaired myelination, IUGR, and microcephaly. Betamethasone is a potent agent, with at least short-term impact on a range of physiologic functions that include endocrine, immune, CV, and neurologic functions. The fetal heart rate pattern may become transiently nonreactive. Intellectual and motor development and school achievement are not adversely influenced by steroid treatment. Some suggest emotional stress during organogenesis might cause congenital defects by increasing the level of endogenous cortisone. Epidemiologic studies report an association between oral clefting and exposure to corticosteroids during organogenesis. After controlling for 4 confounding factors, it was concluded prenatal exposure increased 94 the risk for cleft lip with or without cleft palate 6-fold. IUGR and shortening of the head and mandible are also suggested as sequelae of chronic steroid use during pregnancy, though it is difficult to separate drug from disease impact. The Collaborative Perinatal Project followed women treated during the 1st trimester. While the number of exposures was limited, no increase in congenital malformations was detected. There was no increase in risk of anomalies when steroids were initiated after organogenesis. Women exposed to topical cortisone during

Pregnancy

have no significant increase in birth defects. Female rats exposed to cortisone in utero exhibit premature vaginal opening. Cortisone accelerates fetal rat intestinal maturation, perhaps explaining why corticosteroids decrease the incidence of NEC. In sum, the evidence that cortisone is a human teratogen is wea

Breastfeeding

There are no adequate reports or well-controlled studies in Breastfeeding women. Cortisone is present in human milk, but it is unclear whether maternal treatment with betamethasone increases the concentration.

Pregnancy

. The absorption level of topical betamethasone is unlikely to have significant systemic effect when applied topically in small amounts.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Considering the dose and route, it is unlikely the maternal systemic concentration will reach clinically relevant level.

Breastfeeding

There is no published experience with topical betamethasone in pregnancy. However, considering the dose and route, it is unlikely the breastfed neonate would ingest clinically relevant amounts.

Pregnancy

. Betaxolol is a cardioselective b1-adrenergic blocker. There are no adequate reports or well-controlled studies in pregnant women. Clearance is not affected by pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Betaxolol crosses the human placenta rapidly, achieving an F:M ratio approaching unity. A similar concentration is found in the amniotic fluid. There is a negative correlation between gestational age and betaxolol clearance. In rats, betaxolol is associated with miscarriage, IUGR, skeletal and visceral abnormalities, and incomplete descent of the testes.

Breastfeeding

Betaxolol is excreted in the breast milk according to the manufacturer, which reports one nursing infant with Side effects . Though the kinetics remain to be elucidated, caution should be exercised when administered in nursing mothers.

Pregnancy

. There are no adequate reports or well-controlled studies of bethanechol in pregnant women. It has been used for decades for the treatment of postpartum urinary retention.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether bethanechol crosses the human placenta.

Breastfeeding

There is no published experience in nursing women. It is unknown whether bethanechol enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of biperiden in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in animal or human fetuses. Biperiden apparently crosses the human placenta, though the kinetics remain to be elucidated.

Breastfeeding

There is no published experience in nursing women. It is unknown whether biperiden enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of bismuth subsalicylate in pregnant women. Stool darkening should not be confused with melena. The long clinical experience with this OTC agent is reassuring.

Fetal Health

Bismuth subsalicylate is minimally absorbed across the gastric mucosa. Bismuth ion is not transported across the placenta. No adverse fetal outcomes have been reported.

Breastfeeding

Bismuth ion is not excreted into breast milk to any significant degree. Excretion of large amounts of bismuth subsalicylate is unlikely considering the lack of systemic absorption.

Pregnancy

. There is limited published experience with bisoprolol during pregnancy.

Fetal Health

There is a single case report of a child with cleft lip/palate and hypoplastic toes born to a woman ingesting multiple agents during pregnancy, including bisoprolol, naproxen, and sumatriptan. It is unknown whether bisoprolol crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether bisoprolol enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Neutropenia is an important risk. Long-term effects of bleomycin on reproductive function are insufficiently studied. Several studies concluded that subsequent fertility is clinically unaffected after treatment.

Fetal Health

There are no adequate reports or well-controlled studies in the human fetus. It is unknown whether bleomycin crosses the human placenta. Neonatal leukopenia has been reported shortly after delivery. Long-term follow-up of children exposed in utero has not revealed abnormalities. Bleomycin is teratogenic in rodents (skeletal malformations, hydroureter, vascular disruptions).

Breastfeeding

There is no published experience in nursing women. It is unknown whether bleomycin enters human breast milk. For that reason, it is usually recommended the drug be discontinued in nursing women.

Pregnancy

. There are no adequate reports or well-controlled studies of bretylium in pregnant women. The one case report chronicled an uncomplicated course after chronic treatment of prolonged QT syndrome.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether bretylium crosses the human placenta.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether bretylium enters human breast milk. The one case report noted no neonatal difficulties.

Pregnancy

. Oral or topical combinations of potassium and sodium bromide significantly improve seborrheic dermatitis and dandruff after 10 weeks. There are no adequate reports or well-controlled studies in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. IUGR, microcephaly, neonatal bromide intoxication (poor suck, weak cry, diminished Moro reflex, lethargy, hypotonia), rash, and sedation are reported after oral use. It is unlikely the maternal systemic concentration will reach a clinically relevant level after topical application.

Breastfeeding

Bromides enter human breast milk. It is unlikely the breastfed neonate would ingest clinically relevant amounts after topical application. The American Academy of Pediatrics considers bromides compatible with breastfeeding.

Pregnancy

. Medical therapy with bromocriptine is the initial treatment of choice for infertility. When this is the primary indication for treatment, bromocriptine use has an extensive safety experience and is preferred by some clinicians. Indeed, most information regarding bromocriptine during

Pregnancy

comes from women treated for infertility with an average duration of exposure of 28d. No special maternal considerations are reported. Bromocriptine is used in many countries for the suppression of breast engorgement after delivery. However, rebound engorgement is common after cessation. In 1994, the FDA withdrew approval for that indication after a series of reports describing severe vasospastic events including stroke, MI, cerebral edema, convulsions, and puerperal psychosis. Recent reports suggest a role in the treatment of peripartal cardiomyopathy and SLE.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether bromocriptine crosses the human placenta. There are no reports of associated malformations after 1st trimester exposure. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Bromocriptine reduces lactation, and its use is generally considered contraindicated during breastfeeding.

Pregnancy

. Bromodiphenhydramine is a diphenhydramine derivative. There are no adequate reports or well-controlled studies in pregnant women. When combined with droperidol, bromodiphenhydramine has been advocated as effective in hospital treatment of severe hyperemesis. Overdose is associated with uterine contractions. It is inferior to nalbuphine for the relief of pruritus associated with intrathecal morphine.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Bromodiphenhydramine crosses the human placenta, but the kinetics remain to be detailed. In sheep, transfer is rapid and directly dependent on gestational age. Maternal drug ingestion during rodent

Pregnancy

may alter physical and reflex development. Rodent teratogenicity studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. 106

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Bromodiphenhydramine is probably excreted into human breast milk.

Pregnancy

. Asthma can be a serious problem during pregnancy. Inhaled corticosteroids should generally be considered the prophylactic medication of choice in pregnant women with persistent asthma, unless well controlled by either cromolyn or nedocromil. Although there are no adequate reports or well-controlled studies of budesonide during pregnancy, it is considered a first-line agent along with beclomethasone. 107

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether budesonide crosses the human placenta. Epidemiologic study suggests budesonide is not a clinically significant teratogen. It appears, though, to cross the mouse placenta, where budesonide increases fetal loss, IUGR, and malformations. Rodents as a group are more susceptible to steroids than humans.

Breastfeeding

There is no published experience in nursing women. It is unknown whether budesonide enters human breast milk. Considering <20% of the inhaled dose reaches the systemic circulation, it is unlikely clinically relevant concentrations will enter the breast milk and be absorbed orally.

Pregnancy

. There is no published experience with bumetanide during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether bumetanide crosses the human placenta. No teratogenic effects were noted in rodent studies. Bumetanide alters in vitro Na2+and Cl?transport across placental membranes.

Breastfeeding

There is no published experience in nursing women. It is unknown whether bumetanide enters human breast milk.

Pregnancy

. Bupivacaine is a very popular agent used for neuraxial anesthesia (epidural or spinal) during labor and delivery alone or in combination with either local anesthetic or narcotic agents. Because of its long duration, it is contraindicated for paracervical block.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Bupivacaine crosses the human placenta, with transfer ratios (agent/antipyrine) in vitro approximating 0.4%. Transfer rate increases as the fetal pH declines. It does cross the rodent placenta (F:M ratio approximating 0.3), and decreased pup survival was reported after treatment with high concentrations.

Breastfeeding

Bupivacaine and its major metabolite are found at clinically irrelevant levels after epidural administration. Though it has not been studied after local infiltration, one-time use is unlikely to pose a clinically significant risk to the Breastfeeding neonate.

Pregnancy

. There is extensive information in the addiction medicine literature concerning the use of opioids in recovering pregnant addicts. Buprenorphine, methadone, and morphine have been used to treat women seeking recovery from opioids, and closely monitored neonatal outcomes have been reassuring.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Buprenorphine crosses the human placenta poorly by a mechanism that does not involve P-glycoprotein. The majority of newborns born to opioid-dependent women show signs of opioid withdrawal. Buprenorphine substitution therapy has been used to prevent neonatal abstinence syndrome (NAS) and poor neurodevelopmental outcome in these infants, and may be less severe than that with methadone, perhaps because of a low placental transfer rate. The NAS associated with buprenorphine appears 12-48h after birth, peaks in 72-96h, and lasts for 120-168h. Time of last drug use and frequency of use during the 3rd trimester are important factors associated with drug-positive meconium specimens where concentrations may predict the onset and frequency of NAS. Buprenorphine has no apparent teratogenic effects. Some exposed children may present with transient motor abnormalities, though most probably resolve completely in 85% of cases.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Buprenorphine is excreted into human breast milk in low concentrations (peak 0.18ng/ml for buprenorphine and 0.20ng/ml for norbuprenorphine). In one woman, the daily amount ingested by the neonate was very low (<4mcg), and no withdrawal signs were noted after Breastfeeding was abruptly interrupted.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Bupropion is an effective adjunct for smoking cessation therapy and may be superior to the nicotine patch. It also appears useful for the treatment of postpartum depression. Glaxo-Wellcome maintains an international registry to follow women treated during pregnancy, and caregivers are encouraged to register treated patients.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether bupropion crosses the human placenta. One prospective comparative study of 136 pregnant women taking bupropion conducted 4mo and 1y after delivery revealed no increase in adverse

Pregnancy

outcomes except for an increase in 1st trimester losses. Another study looked at 1200 1st trimester exposures and concluded there was no increase in congenital malformations compared to control. Rodent studies too are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Bupropion is excreted into human breast milk, achieving M:P ratios of 2.5-8.6. However, the neonatal concentration was below the level of detection in the 3 newborns studied. Confirmatory studies are needed.

Pregnancy

. There is no published experience with buspirone during pregnancy. Buspirone interacts with numerous other drugs.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether buspirone crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. In vitro, buspirone reduces neuronal apoptosis after exposure to alcohol.

Breastfeeding

There is no published experience in nursing women. It is unknown whether buspirone enters human breast milk. Buspirone is excreted into rodent breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Busulfan has been used successfully to treat leukemia and essential polycythemia during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether busulfan crosses the human placenta. No pattern of anomalies can be discerned. There are reports of IUGR fetuses born to women who were treated with busulfan during pregnancy. In rodents, there is a high incidence of carpal and tarsal bone anomalies after small doses of antiproliferatives such as cytosine arabinoside, mitomycin C, or busulfan. Further, infertility may be increased in the offspring of treated rats. 116

Breastfeeding

There is no published experience in nursing women. It is unknown whether busulfan enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of butalbital in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in animal and human fetuses. It is unknown whether butalbital crosses the human placenta. Other barbiturates do cross. Withdrawal seizures have been reported in neonates whose mothers used butalbital during pregnancy.

Breastfeeding

There is no published experience in nursing women. It is unknown whether butalbital enters human breast milk. Other barbiturates enter human breast milk, but the kinetics are poorly described.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women prior to 37w. Butorphanol provides better initial analgesia than fentanyl during labor with fewer patient requests for more medication or epidural analgesia. In one well- designed study, it was less effective than meperidine for the relief of affective pain during labor. Acute psychosis has been reported after usage.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Butorphanol crosses the human placenta, achieving an F:M ratio approximating unity. Its use during labor is associated with a transient (90-120min) sinusoidal fetal heart rhythm. The addition of butorphanol, fentanyl, or sufentanil to epidural bupivacaine (0.25%) does not alter FHR short- or long-term variability. Neonatal respiratory depression may occur after parenteral maternal administration. No teratogenic effects are identified in rodents.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Butorphanol is excreted into human breast milk, but it is estimated the unsupplemented neonate would ingest 4mcg/d if the woman was receiving an analgesic dose (2mg IM or 8mg PO) 4?/d.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Cabergoline is better tolerated and more effective in inducing a complete biochemical response than bromocriptine. Women become pregnant in 1-37mo (mean 12.4mo) with cabergoline therapy. It has been used successfully throughout

Pregnancy

to treat a macroprolactinoma; most tumors disappear with therapy. Cabergoline is also effective in women resistant or poorly responsive to bromocriptine. Prolactin typically trends lower after delivery or 3mo after breastfeeding. Cabergoline is used in several countries to prevent postpartum lactation (1mg PO ?1) or block established lactation (0.25mg PO q12h ?4).

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cabergoline crosses the human placenta. First trimester exposure is not associated with adverse perinatal outcome. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether cabergoline enters human breast milk. Cabergoline effectively suppressed lactation in some studies, with less rebound than bromocriptine. It should be avoided if Breastfeeding is desired.

Pregnancy

. There is no clear evidence caffeine at moderate ingestion levels has an adverse effect on pregnancy. Toxicity occurs only in very high dosages (e.g., 25 tablets of Fiorinal [ASA, butalbital, caffeine]).

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Caffeine crosses the placenta, achieving an F:M ratio near unity. Cardiac arrhythmias are associated with maternal caffeine use in excess of 500mg/d. There is no substantive evidence that caffeine is either a teratogen or causes IUGR in humans. In rodents, high and sustained doses are associated with a small increase in the prevalence of cleft palate. Despite the fact that many epidemiologic studies observed a positive association between maternal caffeine intake and the risk of spontaneous abortion, the evidence is still equivocal given the biases likely present and the fact that most of the potential biases would overestimate any association.

Breastfeeding

Though it enters human breast milk in small amounts, caffeine is generally considered safe for Breastfeeding women.

Pregnancy

. There are only scattered case reports of Cafergot use during pregnancy. This combination is contraindicated due to the oxytocic effects of ergotamine. See caffeine and ergotamine individually.

Fetal Health

See caffeine and ergotamine individually. Jejunal atresia was reported in the child of a woman who ingested Cafergot in 5 consecutive pregnancies. The other 4 ended in spontaneous abortion.

Breastfeeding

There is no published experience in nursing women. See caffeine and ergotamine individually.

Pregnancy

. Vitamin D supplementation is recommended during pregnancy. Calcifediol is converted in the kidney to an active form of vitamin D, calcitriol. There are no adequate reports or well- controlled studies in pregnant women. Veiled or dark-skinned pregnant women have an increased risk of vitamin D deficiency, which is associated with disease.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. There is a weak association between vitamin D levels and gestational age and fetal heel length. It is unknown whether calcifediol crosses the human placenta, though the placenta synthesizes active vitamin D. Calcifediol is reportedly teratogenic in some rodents.

Breastfeeding

There is no published experience in nursing women. It is unknown whether calcifediol enters human breast milk, but supplementation has little effect on milk vitamin D levels.

Pregnancy

. Calcitonin regulates calcium homeostasis. There are no adequate reports or well-controlled studies in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in pregnant women. Calcitonin does not cross the placenta. The mechanism by which high doses of calcitonin produce IUGR in rabbits is unknown.

Breastfeeding

There is no published experience in nursing women. Calcitonin inhibits lactation in animals. It is unknown whether calcitonin enters human breast milk, though the high molecular weight argues against it. Further, any calcitonin in the milk would be destroyed by gastric acid. Procalcitonin is a normal constituent of human breast milk.

Pregnancy

. Calcitriol is an active form of vitamin D. There are no adequate reports or well-controlled studies in pregnant women. Vitamin D supplementation is recommended during pregnancy. Calcitriol combined with calcium supplementation helps lower systolic BP in older women.

Fetal Health

There are no adequate reports or well-controlled studies of the effect of calcitriol in human fetuses. It is unknown whether calcitriol crosses the human placenta, though the placenta synthesizes active vitamin D. Calcitriol is reportedly teratogenic in rabbits but not rats.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether calcitriol enters human breast milk, but supplementation has little effect on milk vitamin D levels.

Pregnancy

. Calcium chloride is lifesaving in women with hypermagnesemia. It provides approximately 3more calcium than calcium gluconate. Calcium chloride reduces the incidence of parturient paresis in cows and transiently increases cardiac output in gravid ewes during hemorrhagic hypotension.

Fetal Health

It is unlikely calcium administration increases the fetal concentration. Calcium chloride decreases the aspirin toxicity in pregnant rats.

Breastfeeding

It is unknown whether calcium chloride supplementation increases calcium concentration in breast milk.

Pregnancy

. The FDA states that OTC drug products may not exceed camphor concentrations of 11%. There are no adequate reports or well-controlled studies in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Camphor crosses the placenta, but there is no evidence of embryo toxicity or teratogenicity.

Breastfeeding

There is no published experience in nursing women. It is unknown whether camphor enters human breast milk. Considering the route and dose, it is unlikely the Breastfeeding neonate would ingest a clinically significant amount.

Pregnancy

. The published experience for candesartan during

Pregnancy

is limited to a few case reports. It is assumed the effects of candesartan are similar to other ACEI class agents. As such, it should be avoided throughout

Pregnancy

unless there is no other option. The lowest dose effective should be used when candesartan is required for BP control during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Candesartan presumably crosses the human placenta since fetal renal effects are reported and other ACEIs cross. AT-1 receptors are expressed on many organs of the human fetus. ACEIs are considered both teratogenic and fetotoxic. They are contraindicated throughout

Pregnancy

as all members of this class may cause cranial hypoplasia, reversible or irreversible renal failure, oligohydramnios, anuria, death, prematurity, IUGR, and patent ductus arteriosus.

Breastfeeding

There is no published experience in nursing women. It is unknown whether candesartan enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of captopril in pregnant women. ACEIs are contraindicated across gestation unless there is no option. Improved

Pregnancy

outcome was noted in diabetic mothers treated prenatally with low doses of captopril. The lowest dose effective should be used when captopril is required during pregnancy. Close monitoring of AF and fetal well-being is recommended.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Captopril apparently crosses the human placenta, though the kinetics remain to be elucidated. ACEIs are considered both teratogenic and fetotoxic. They are contraindicated throughout

Pregnancy

as all members of this class may cause cranial hypoplasia, reversible or irreversible renal failure, oligohydramnios, anuria, death, prematurity, IUGR, and patent ductus arteriosus. Captopril is embryocidal and causes stillbirths in a variety of animals (sheep, rabbits, rats).

Breastfeeding

Captopril is excreted in breast milk at a very low concentration and is generally considered compatible with breastfeeding. 130

Pregnancy

. There are no adequate reports or well-controlled studies of the effect of carbachol in pregnant women. Carbachol is a potent stimulator of myometrial contractility in rodents. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether carbachol crosses the human placenta. Considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level.

Breastfeeding

There is no published experience in pregnancy. It is unknown whether carbachol enters human breast milk. However, considering the dose and route, it is unlikely the breastfed neonate would ingest a clinically relevant amount.

Pregnancy

. Anticonvulsant drugs should not be discontinued abruptly during

Pregnancy

if used to prevent seizures, as there is a significant possibility of precipitating status epilepticus. There are no adequate reports or well-controlled studies of carbamazepine in pregnant women. It would seem advisable for women to continue medication during

Pregnancy

using monotherapy at the lowest dose required to achieve seizure control. Polytherapy would seem best avoided where possible.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Carbamazepine rapidly crosses the human placenta and accumulates in fetal organs, including the brain. Epidemiologic study suggests carbamazepine is a teratogen causing facial dysmorphism, spina bifida, distal phalange hypoplasia, and developmental delay. In prospective studies involving 1255 exposures, carbamazepine was associated with increased rates of neural tube, CV, urinary tract, and cleft palate anomalies. One overview (Cochrane) concluded the evidence is weak that carbamazepine is a teratogen as monotherapy. More recent epidemiologic evidence, however, concludes carbamazepine is a modest teratogen?less than phenytoin, but more than other anticonvulsant agents. The combination of carbamazepine with other antiepileptic drugs has a synergistic effect on the prevalence of birth defects. There is also concern that carbamazepine exposure increases the risk of neonatal intracranial hemorrhage. Rodent studies reveal an increased prevalence of talipes, cleft palate, and anophthalmos.

Breastfeeding

Carbamazepine is excreted in human breast milk. Although it is generally considered safe for Breastfeeding women, neonatal sequelae reported include cholestatic hepatitis. The infant should 133 be monitored for possible adverse effects, the drug given at the lowest effective dose, and

Pregnancy

. Carbenicillin is indicated for the treatment of acute and chronic infections of the upper and lower urinary tract. There are no adequate reports or well-controlled studies in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether carbenicillin crosses the human placenta. Other penicillins do cross to varying degrees. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. Carbenicillin is excreted into breast milk in low concentrations, but is generally considered safe during breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of carbidopa in pregnant women.

Pregnancy

may exacerbate Parkinson?s disease and have a long-term negative impact on the course of the illness.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Carbidopa crosses the rat and human placenta, and the fetal blood-brain barrier. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Its use with levodopa is associated with visceral and skeletal malformations in rabbits.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether carbidopa enters human breast milk.

Pregnancy

. There is no published experience with carbinoxamine during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether carbinoxamine crosses the human placenta.

Breastfeeding

There is no published experience in nursing women. It is unknown whether carbinoxamine enters human breast milk.

Pregnancy

. Carboprost is an analog of 15-methylprostaglandin PGF2a. It is a second-line agent for the treatment of uterine atony refractive to oxytocin behind methergine/ergotrate because of the high incidence of GI complaints (21% vs <1%). Some suggest that it is more effective if given directly into the myometrium, but there are no trial data to support the practice. Carboprost has also been given both IM and intra-amniotically for

Pregnancy

termination, though both misoprostil and PGE2are superior for this indication. It can speed cervical ripening (200mcg IM), but once administered may be difficult to control. Misoprostil is superior for preparation for a 1st trimester vacuum aspiration.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether carboprost crosses the human placenta. The principal risk reflects that of hypoxia associated with uterine tachysystole.

Breastfeeding

There is no published experience in nursing women. It is unknown whether carboprost enters human breast milk.

Pregnancy

. The major metabolite of carisoprodol is meprobamate. There are no adequate reports or well-controlled studies in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Carisoprodol crosses the human placenta and in limited study, does not appear to cause developmental toxicity. Rodent teratogenicity studies have not been performed.

Breastfeeding

Carisoprodol is concentrated in breast milk. The absolute dose ingested by an exclusively breastfed infant was estimated at 1.9mg/kg/d, and the relative dose 4.1% of the weight-adjusted maternal dose. No adverse effects are reported.

Pregnancy

. There is no published experience with carteolol during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies of carteolol in human fetuses. Rodent studies are reassuring, revealing no evidence of teratogenicity despite the use of doses dramatically higher than those used clinically. There was, however, evidence of fetotoxicity and IUGR at these high doses.

Breastfeeding

There is no published experience in nursing women. It is unknown whether carteolol enters human breast milk. It does enter rat milk.

Pregnancy

. There are no adequate reports or well-controlled studies of carvedilol in pregnant women. There are reports of its use for the treatment of peripartal cardiomyopathy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether carvedilol crosses the human placenta. Carvedilol crosses the rodent placenta, and produces fetotoxicity and IUGR when given in doses that are multiples of the MRHD.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether carvedilol enters human breast milk. It does enter the milk of some rodent species.

Pregnancy

. There are no adequate reports or well-controlled studies of casanthranol in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether casanthranol crosses the human placenta. It is not associated with an increased incidence of fetal malformations. Rodent teratogenicity studies have apparently not been performed.

Breastfeeding

There is no published experience during pregnancy. It is unknown whether casanthranol enters human breast milk. A metabolite, anthraquinone, is excreted into breast milk and may increase the incidence of diarrhea in infants of nursing mothers. However, it is generally considered safe during breastfeeding.

Pregnancy

. Because of its antimicrobial spectrum, cefaclor is used to treat acute bronchitis, pharyngitis, and skin infections. It has poor activity against the anaerobes associated with bacterial vaginosis. There are no adequate reports or well-controlled studies in pregnant women. However, cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cefaclor crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Most cephalosporins are excreted into breast milk. While there are no adequate reports or well-controlled studies in nursing women, cefaclor is generally considered compatible with breastfeeding.

Pregnancy

. Because of its antimicrobial spectrum, cefadroxil is used to treat UTIs and pharyngitis. There are no adequate reports or well- controlled studies in pregnant women. However, cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cefadroxil crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Cefadroxil is excreted into breast milk in low concentrations; it is generally considered compatible with breastfeeding.

Pregnancy

. Because of its antimicrobial spectrum, cefamandole is used to treat lower respiratory tract infections, UTIs, peritonitis, and septicemia and for post?cesarean section prophylaxis. For the latter, it has no advantage over any other cephalosporin. Though used by some for the treatment of group B streptococcus colonization, there is growing resistance. Cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cefamandole crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Cefamandole is excreted into breast milk in low concentrations; it is generally considered safe during breastfeeding.

Pregnancy

. Because of its antimicrobial spectrum, cefazolin is used to treat lower respiratory tract infections, GU tract infections, skin infections, peritonitis, septicemia, and endocarditis; for post- cesarean section prophylaxis; and intrapartum for group B streptococcus. Cefazolin is superior to clindamycin and erythromycin for group B streptococcus prophylaxis in patients with a non-anaphylactic penicillin allergy. The prophylactic administration of cefazolin preoperatively, intraoperatively, or postoperatively reduces the incidence of post?cesarean section infection. The timing of administration does not significantly alter efficacy. For this indication, it has no clinical advantage over any other cephalosporin, and cost is often the deciding factor. Prophylaxis is usually discontinued within 24h of the surgical procedure. Cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cefazolin rapidly crosses the human placenta, achieving concentrations greater than or equal to the 90% MIC for group B streptococcus maternal, fetal, and AF samples. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

While there are no adequate reports or well-controlled studies in nursing women, cefazolin is apparently excreted into human breast milk. Though the kinetics remain to be elucidated, it is generally considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of cefdinir in pregnant women. It appears effective and safe during

Pregnancy

for the treatment of acute infections, but has no unique advantage over other cephalosporins for most indications. Cost is often a key decision factor.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cefdinir crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Most cephalosporins are excreted into breast milk. While there is no published experience in nursing women, cefdinir is generally considered compatible with breastfeeding.

Pregnancy

. There is no published experience with cefditoren during pregnancy. Cephalosporins are generally considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cefditoren crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Most cephalosporins are excreted into breast milk. While there is no published experience in nursing women, cefditoren is generally considered compatible with breastfeeding.

Pregnancy

. Cefepime is used to treat lower respiratory tract infections, GU tract infections, skin infections, and neutropenic patients because of its antimicrobial spectrum. Limited study suggests it is effective as cefotaxime for the treatment of acute obstetric and gynecologic infections. Third- and 4th-generation cephalosporins (e.g., cefotaxime, cefoperazone, ceftriaxone, ceftazidime, ceftizoxime) are generally not recommended for surgical prophylaxis. Despite these recommendations, they have been accepted by the medical community for prophylaxis and are today commonly misused. Cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cefepime crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Most cephalosporins are excreted into breast milk. While there is no published experience in nursing women, cefepime is generally considered compatible with breastfeeding.

Pregnancy

. Cefixime is used to treat lower respiratory tract infections, otitis media, pharyngitis, acute bronchitis, acute exacerbation of chronic bronchitis, gonorrhea, GU tract infections, skin infections, and neutropenic patients because of its antimicrobial spectrum. Cefixime is an effective and safe oral medication during

Pregnancy

for the treatment of acute obstetric diseases and STDs such as gonorrhea. Third- and 4th-generation cephalosporins (e.g., cefotaxime, cefoperazone, ceftriaxone, ceftazidime, ceftizoxime) are generally not recommended for surgical prophylaxis. Despite these recommendations, they have been accepted by the medical community for prophylaxis and are today commonly misused. Cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cefixime crosses the human placenta. Transfer across the rodent placenta is poor. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. 151

Breastfeeding

Most cephalosporins are excreted into breast milk. While there is no published experience in nursing women, cefixime is generally considered compatible with breastfeeding. Transfer into rodent milk occurs at low levels.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Cefmetazole is highly effective against most causes of bacterial vaginosis during pregnancy. Cefmetazole appears equivalent to cefoxitin in reducing post?cesarean section endometritis. Cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cefmetazole rapidly crosses the human placenta, yielding fetal levels in excess of the typical MIC. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Only a scant amount of cefmetazole is excreted into human breast milk, and it is generally considered compatible with breastfeeding.

Pregnancy

. Because of its antimicrobial spectrum, cefonicid is used to treat lower respiratory tract infections, GU tract infections, skin 153 infections, and septicemia and for surgical prophylaxis. It appears effective and safe during

Pregnancy

for the treatment of acute infections and post?cesarean section prophylaxis, but has no unique advantage over other cephalosporins for most indications. Cost is often a key decision factor. Cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cefonicid crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Cefonicid is excreted at low concentrations into human breast milk, but is generally considered compatible with breastfeeding.

Pregnancy

. Because of its antimicrobial spectrum, cefoperazone is used to treat lower respiratory tract infections, GU tract infections, skin infections, and septicemia and for surgical prophylaxis. Cefoperazone appears effective and safe during

Pregnancy

for the treatment of acute infections. Clearance is only modestly affected by pregnancy. Third- and 4th-generation cephalosporins (e.g., cefotaxime, cefoperazone, ceftriaxone, ceftazidime, ceftizoxime) are generally not recommended for surgical prophylaxis. Despite these recommendations, they have been accepted by the medical community for prophylaxis and are today commonly misused.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cefoperazone crosses the human placenta, but to a lower degree than ceftizoxime. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Cefoperazone is excreted in small amounts into human breast milk, and is generally considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of ceforanide in pregnant women. It appears to have no unique advantage over other cephalosporins for most indications. Cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether ceforanide crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Most cephalosporins are excreted into breast milk. While there is no published experience in nursing women, ceforanide is generally considered compatible with breastfeeding.

Pregnancy

. Cefotaxime is used to treat lower respiratory tract infections, GU tract infections, skin infections, and septicemia and for surgical prophylaxis because of its antimicrobial spectrum. Cefotaxime appears effective and safe during

Pregnancy

for the treatment of acute infections. High AF concentrations suggest it may be advantageous for the treatment of chorioamnionitis. Third- and 4th-generation cephalosporins (e.g., cefotaxime, cefoperazone, ceftriaxone, ceftazidime, ceftizoxime) are generally not recommended for surgical prophylaxis. Despite these recommendations, they have been accepted by the medical community for prophylaxis and are today commonly misused.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cefotaxime crosses the human placenta. Though the kinetics remain to be elucidated, it achieves amniotic fluid concentrations that exceed the 90% MIC for most strains of E. coli. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Scant quantities of cefotaxime are excreted into human breast milk, and it is generally considered compatible with breastfeeding. 157

Pregnancy

. Because of its antimicrobial spectrum, cefotetan is used to treat lower respiratory tract infections, GU tract infections, skin infections, septicemia, and surgical prophylaxis. Cefotetan appears effective and safe during

Pregnancy

for the treatment of acute infections. However, it has no activity against Chlamydia trachomatis. When used for the treatment of PID, appropriate antichlamydial coverage should be added. Single-dose cefotetan can replace the multidose cefoxitin regimen for post?cesarean section prophylaxis with considerable cost savings. Case reports 158 describe maternal hemolysis associated with cefotetan for post?cesarean section prophylaxis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cefotetan crosses both rodent and human placentas, though the kinetics remain to be elucidated. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

While there are no adequate reports or well-controlled studies in nursing women, cefotetan is excreted in scant quantities into human breast milk and is generally considered compatible with breastfeeding.

Pregnancy

. Cefoxitin is used to treat lower respiratory tract infections, GU tract infections, skin infections, and septicemia and for surgical prophylaxis because of its antimicrobial spectrum. It is a preferred agent for the treatment of PID where inpatient and outpatient therapy (combined with doxycycline) yield similar results. Cefoxitin appears effective and safe during

Pregnancy

for the treatment of acute infection, though there are more cost- effective regimens for post?cesarean section prophylaxis. It is not beneficial for elective cesarean delivery.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cefoxitin crosses the human placenta, achieving an F:M ratio approximating 0.6 at 45min after maternal injection. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Most cephalosporins are excreted into breast milk. There is little detectable cefoxitin in human breast milk after post?cesarean section prophylaxis. It is generally considered compatible with breastfeeding.

Pregnancy

. There is little published experience with cefpodoxime during pregnancy. Third- and 4th-generation cephalosporins are generally not recommended for surgical prophylaxis. Despite these recommendations, they have been accepted by the medical community for prophylaxis and are commonly misused. Cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cefpodoxime crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Most cephalosporins are excreted into breast milk. While there is no published experience in nursing women, cefpodoxime reportedly is excreted in breast milk at modest levels. The kinetics remain to be detailed.

Pregnancy

. There is no published experience with cefprozil during pregnancy. Cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cefprozil crosses the human placenta. Small quantities cross the rodent placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Cefprozil is excreted into human breast milk in very small quantities, but even if one assumes the concentration in milk remains constant at the highest observed, a neonate ingesting an average of 800ml of milk/d would ingest a maximum of about 3mg of cefprozil/d. 162

Pregnancy

. Ceftazidime is a 3rd-generation cephalosporin that retains a broad spectrum of in vitro antimicrobial activity and clinical utility in serious infections, particularly those due to major nosocomial pathogens, and respiratory infections in patients with cystic fibrosis. Ceftazidime-containing regimens are important for febrile episodes in neutropenic patients. There are no adequate reports or well-controlled studies of ceftazidime in pregnant women. Maternal renal elimination is increased during pregnancy, and the dose may need adjustment to achieve 163 therapeutic levels. Third- and 4th-generation cephalosporins are not generally recommended for surgical prophylaxis. Despite these recommendations, they have been accepted by the medical community for prophylaxis and are today commonly misused.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Ceftazidime crosses the human placenta, achieving an F:M ratio in the 2nd trimester approximating 0.15, and a M:AF ratio of 0.19. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Ceftazidime is excreted into human breast milk in very small quantities, but even if one assumes the concentration in milk remains constant at the highest observed, a neonate ingesting an average of 800ml of milk/d would ingest a maximum of about 4mg of ceftazidime/d.

Pregnancy

. Ceftibuten is effective treatment for acute UTI during pregnancy. There is little experience during

Pregnancy

with other indications. Third- and 4th-generation cephalosporins are not generally recommended for surgical prophylaxis. Despite these recommendations, they have been accepted by the medical community for prophylaxis and are today commonly misused. Cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether ceftibuten crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Most cephalosporins are excreted into breast milk. However, the concentration of ceftibuten in breast milk is minimal and considered compatible with breastfeeding.

Pregnancy

. Ceftizoxime appears effective and safe for the treatment of acute infections during pregnancy. It has no effect on the interval to delivery, or the duration of

Pregnancy

in women treated for preterm labor with intact membranes. Third- and 4th-generation cephalosporins are not generally recommended for surgical prophylaxis. Despite these recommendations, they have been accepted by the medical community for prophylaxis and are today commonly misused. Cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Ceftizoxime concentrations are higher in cord blood and AF than in maternal blood, perhaps because of more avid binding to fetal serum proteins. It is the only antibiotic known to have such high transfer. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Most cephalosporins are excreted into breast milk, but the amount of ceftizoxime excreted is minimal and generally considered compatible with breastfeeding.

Pregnancy

. Ceftriaxone appears effective and safe during

Pregnancy

for the treatment of acute infections. Ceftriaxone (single dose given IM) is a drug of choice for the treatment of gonorrhea in pregnancy. 167 A single dose is as effective for post?cesarean prophylaxis as 3 doses of ampicillin/cloxacillin. However, 3rd- and 4th-generation cephalosporins are not generally recommended for surgical prophylaxis. Despite these recommendations, they have been accepted by the medical community for prophylaxis and are today commonly misused. Cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Ceftriaxone rapidly crosses the human placenta, reaching therapeutic concentrations in the fetal compartments. Some studies suggest that intrapartum prophylaxis with ceftriaxone decreases the rates of bacterial colonization and early- onset infection in newborns. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. However, ceftriaxone weakly impairs in vitro rat nephrogenesis at all doses studied except 1000mcg/ml, which blocked kidney development completely.

Breastfeeding

Most cephalosporins are excreted into breast milk, but the amount of ceftriaxone excreted is <5% of a 2g maternal dose. It is generally considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of cefuroxime in pregnant women. It appears to be safe and effective during

Pregnancy

for the treatment of acute infections, especially pyelonephritis. One investigator suggested it was a first- choice option for the treatment of acute pyelonephritis during

Pregnancy

due to its tolerance, microbiologic activity, and superior clinical effect compared to cephradine. Cephalosporins are usually considered safe during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cefuroxime crosses the human placenta at a rate unaffected by gestational age and anemia, but requires a dose of at least 1500mg to achieve the typical MIC in the fetus. Bactericidal concentrations can be demonstrated in maternal plasma and in AF leaking from the vagina. A concentration-time curve in AF occurs, with peak concentrations 3-4h after infusion. Therapeutically active levels are present in the newborns. The resorption of cefuroxime by the fetal membranes is high. There is no evidence of teratogenicity after 1st trimester exposure, and children of women treated with cefuroxime are normal at 18mo. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. 169

Breastfeeding

Most cephalosporins are excreted into breast milk. While there are no adequate reports or well-controlled studies in nursing women, cefuroxime is generally considered compatible with breastfeeding.

Pregnancy

. Celecoxib is the prototype COX-2 inhibitor. There are no adequate reports or well-controlled studies in pregnant women. 170 In vitro studies reveal inhibition of uterine contractions by COX- 2 inhibition. In two small trials, celecoxib was employed as a tocolytic agent with modest effect. Celecoxib (80 and 160mg/kg/ d) significantly reduces fertility, prolongs pregnancy, and inhibits normal cervical ripening in rats. The authors concluded it was similar to indomethacin but with a lower frequency of adverse fetal effects. However, in a series of recent studies, COX-2 inhibition was associated with a dose-related increase in death from CV causes, MI, stroke, or heart failure. In light of these reports, celecoxib use should be avoided for most indications in favor of other agents especially in women with CV and GI risks.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Celecoxib crosses the human placenta, as do other NSAIDs, and can cause ductus arteriosus constriction late in pregnancy. Fetal levels are dependent on the maternal concentrations because NSAID agents are not metabolized by the fetal kidney. It reduces renal blood and urine flows in the ovine fetus. Celecoxib increases the incidence of VSD and other fetal alterations such as fused ribs and misshapen sternum in rabbits treated during organogenesis. There is a dose-dependent increase in the frequency of diaphragmatic hernia in rats.

Breastfeeding

There are no adequate reports or well-controlled studies of celecoxib in nursing women. A single case report found a concentration of 133ng/ml approximately 5h after a 100mg dose and an elimination t/2 of 4.0-6.5h. If this level were sustained, the amount ingested by a 3.5kg newborn in 24h should be subclinical.

Pregnancy

. Cephalexin is used for the treatment of UTIs, acute obstetric infections, and pharyngitis because of its antimicrobial spectrum. Cephalexin appears effective and safe during

Pregnancy

for the treatment of acute bacterial infection. It is extensively used for the oral phase of treatment for pyelonephritis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cephalexin crosses the human placenta in a carrier-mediated fashion. The magnitude of transfer is greater than cephapirin, and produces a fetal concentration above the MIC for most sensitive pathogens. There is no evidence of teratogenicity. Rodent studies are also reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Most cephalosporins are excreted into breast milk, but the amount of cephalexin excreted is small and generally considered compatible with breastfeeding.

Pregnancy

. The elimination t/2 of this 1st-generation cephalosporin is reduced by1=3 during pregnancy. Primary treatment of UTIs with a 1st-generation cephalosporin during

Pregnancy

may no longer be appropriate in some geographic locales as a significant number of isolates (11%) are resistant to cephalothin. Prophylactic cephalothin decreases the incidence of endometritis in women undergoing midtrimester abortion and cesarean section as well as do other cephalosporins.

Fetal Health

There are no adequate reports or well-controlled studies of cephalothin in human fetuses. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Most cephalosporins are excreted into breast milk, but the amount of cephalothin excreted is small and generally considered compatible with breastfeeding.

Pregnancy

. Cephapirin appears effective and safe for the treatment of acute infection during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cephapirin crosses the human placenta, and though the magnitude of transfer is less than cephalexin, it does produce a fetal concentration above the MIC for most sensitive pathogens. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Most cephalosporins are excreted into breast milk, but the amount of cephapirin excreted is small and generally considered compatible with breastfeeding.

Pregnancy

. Cephradine has been used for the treatment of UTI and pharyngitis because of its antimicrobial spectrum. However, its elimination t/2 is decreased by 25% during pregnancy, which might in part explain why cefuroxime proved superior in one randomized trial for the treatment of UTI.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cephradine rapidly crosses the human placenta and is found in the AF within hours of maternal administration. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. 176

Breastfeeding

Cephradine is excreted into human breast milk. Its M:P ratio approximates 0.2, suggesting cephradine should be compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of cetirizine in pregnant women. The product labels state medications for allergic rhinitis should be avoided during

Pregnancy

owing to lack of fetal safety, though the majority of agents have human data that refute this position. In general, treatment of allergic rhinitis during

Pregnancy

should begin with the 1st-generation antihistamines, chlorpheniramine and tripelennamine. Pregnant women who cannot tolerate 1st- generation antihistamines may be offered a 2nd-generation agent, either loratadine or cetirizine.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cetirizine crosses the human placenta. Neither 1st- (e.g., chlorpheniramine) nor 2nd-generation (e.g., cetirizine) antihistamines are incriminated as human teratogens. Though 1st trimester exposure studies are reassuring, 1st-generation antihistamines are preferred as there is more conclusive evidence of safety. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Cetirizine enters human breast milk, though the kinetics remain to be elucidated.

Pregnancy

. Because of potential hepatotoxicity, poor response rates in some subgroups of chenodiol-treated patients, and an increased cholecystectomy rate in other treated subgroups, chenodiol is not appropriate treatment for many patients with gallstones. There are no adequate reports or well-controlled studies of chenodiol in pregnant women. Maternal

Pregnancy

outcome may be improved in pregnancies complicated by intrahepatic cholestasis by treatment with ursodeoxicholic acid.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown if chenodiol crosses the placenta. Bile acid levels are lower in both AF and umbilical blood samples from pregnancies treated for intrahepatic cholestasis with ursodeoxicholic acid, suggesting placental transfer. Serious hepatic, renal, and adrenal lesions occurred in rhesus fetuses given 60-90mg/kg/d (4-6the MRHD) from day 21 to day 45 of pregnancy. Hepatic lesions occurred in neonatal baboons whose mothers received 18-38mg/kg (1-2the MRHD) throughout pregnancy. Fetal malformations were not observed. Neither fetal liver damage nor fetal abnormalities occurred in reproduction studies in rats and hamsters.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether chenodiol enters human breast milk.

Pregnancy

. Chloral hydrate is an anxiolytic hypnotic. There are no adequate reports or well-controlled studies in pregnant women. There is a case report of successful hemodialysis during

Pregnancy

for the treatment of a chloral hydrate overdose.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Chronic use during

Pregnancy

may result in neonatal withdrawal, suggesting placental transfer. Rodent teratogenicity studies have apparently not been performed. Equine studies suggest a higher frequency of miscarriage after chloral hydrate.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Chloral hydrate is excreted into human breast milk and may cause neonatal sedation.

Pregnancy

. Chlorambucil is an alkylating agent used in chemotherapy protocols for many malignant diseases, including gestational trophoblastic disease and ovarian cancer. There are no adequate reports or well-controlled studies in pregnant women. There are many case reports of a successful outcome in women treated with chlorambucil throughout pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in animal and human fetuses. It is unknown whether chlorambucil crosses the human placenta. The sole report of a chlorambucil- associated birth defect is unilateral renal agenesis in 1 fetus of a set of twins. The lack of reports suggests chlorambucil is not a major human teratogen, and fetal tolerance later in gestation is quite high. Chlorambucil is a teratogen in rodents, causing postclosure exencephaly and axial skeletal abnormalities.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether chlorambucil enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of chloramphenicol in pregnant women. It has been used for the treatment of rickettsial disease, also known as scrub typhus.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether chloramphenicol crosses the human placenta. Thiamphenicol does cross the rodent placenta. Chloramphenicol is not teratogenic in either humans or rodents. It does cause neonatal gray baby syndrome. Case reports document successful treatment of meningoencephalitis in neonates caused by maternal Mycoplasma hominis.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Chloramphenicol enters human breast milk, but the levels achieved appear low, ranging from 0.54 to 2.84mg/L in women taking 250mg PO qid, and 1.75-6.10mg/L in women taking 500mg PO qid. The M:P ratio range is between 0.53 and 0.84. Yet, caution is advised in nursing mothers treated systemically due to the danger of gray baby syndrome in neonates.

Pregnancy

. There are no adequate reports or well-controlled studies of chlordiazepoxide during pregnancy. The available information is insufficient to determine whether the potential benefits of benzodiazepines to the mother outweigh the risks to the fetus. High peak concentrations are avoided by dividing the daily dosage into 2 or 3 doses.

Fetal Health

Benzodiazepines are rapidly transferred across the placenta during early and late pregnancy, and 1st trimester exposure to this class of drugs has been linked to an increased risk of anomalies. While there are no well-controlled studies of chlordiazepoxide in human fetuses, the overall experience has been reassuring. In some 550 children followed up to 4y, there was no increase in either malformations or adverse effects on neurobehavioral development and IQ. Some infants exposed in the 3rd trimester exhibit either the floppy infant syndrome or marked neonatal withdrawal symptoms. Symptoms vary from mild sedation, hypotonia, and reluctance to suck to apneic spells, cyanosis, and impaired metabolic responses to cold stress, and may persist for hours to months after birth. This correlates with the pharmacokinetic and placental transfer of the benzodiazepines and their disposition in the neonate. Chlordiazepoxide retards motor development and physical maturation in mice. Rodent studies reveal no increased risk of congenital anomalies, IUGR, or adverse effects on lactation.

Breastfeeding

There are no adequate reports or well-controlled studies of chlordiazepoxide in nursing women. The drug enters human 184 breast milk in low concentrations such that only high clinical doses might be expected to exert an effect on the nursing newborn.

Pregnancy

. While there are no adequate reports or well-controlled studies in pregnant women, chlorhexidine is considered safe for cleansing of the birth canal, and may be as effective as ampicillin for the prevention of neonatal group B streptococcus. Some studies suggest its use during labor may also decrease HIV transmission. It does not, however, reduce the incidence of postpartum endometritis.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether chlorhexidine crosses the 185 human placenta. Exposure to chlorhexidine during birth is not associated with any increase in neonatal mortality rate due to sepsis, fever, poor feeding, apnea, or dyspnea in newborns.

Breastfeeding

It is not known whether chlorhexidine enters human milk. While there are no adequate reports or well-controlled studies in nursing women, the quantity of drug absorbed systemically during a brief encounter is likely minimal.

Pregnancy

. Chloroquine is closely related to hydroxychloroquine and has similar uses. A body of clinical experience suggests chloroquine is safe during

Pregnancy

and improves outcome in women with active disease. In one study of 96 women with active malaria, chloroquine (10mg/kg) was given at time 0 and 24h and again at 48h (5mg/kg). The Tmaxafter the first dose was 3.5h, whereas plasma concentrations (CPmax) at 2, 28, and 52h were 204.36, 343.51, and 257.04ng/ml respectively. There was total parasitemia clearance before the end of 96h in all the subjects. In another study, the conversion of chloroquine to its major metabolite, desethylchloroquine, was increased in the 3rd trimester, suggesting the need for caution when considering the use of higher doses. Current study suggests there are more effective treatment options. Chloroquine is also used as an adjunct for the treatment of SLE in women who have failed to respond to first-line agents. Recent studies suggest it may have a role in the treatment of HIV, and thus may have a role in HIV-infected Side effects include agranulocytosis, thrombocytopenia, aplastic anemia, dermatitis, ototoxicity, vomiting, dizziness, diarrhea, and pruritus.

Fetal Health

Chloroquine crosses the placenta, achieving an F:M ratio approximating 0.7-0.8. Fetal retinopathy was noted in some animal studies, but more recent investigation casts doubt on the association and suggests it is safe during the 1st trimester. No increase in spontaneous abortion or major birth defects is reported in humans. Breastfeeding Chloroquine enters human breast milk, achieving an M:P ratio ranging from 0.268 to 0.462. Some studies suggest it may actually be concentrated. However, it is generally considered compatible with breastfeeding.

Pregnancy

. Though popular among obstetricians for the treatment of edema and weight gain in the 1970s, there are no adequate reports or well-controlled studies of chlorothiazide in pregnant women. Physiologic edema should not be treated. Thiazide diuretics may be diabetogenic. Severe electrolyte imbalances in both mother and newborn are reported. Hemorrhagic pancreatitis is also reported after thiazide exposure.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Thiazide diuretics readily cross the placenta. There is no clear evidence chlorothiazide increases the risk of malformation. However, older studies suggest thiazide diuretics may decrease placental perfusion by preventing normal plasma expansion and increase the risk of IUGR. Thrombocytopenia and hypoglycemia are major risks. The mechanism for the thrombocytopenia is unknown. Fetal bradycardia following exposure is the result of electrolyte imbalance (hypokalemia).

Breastfeeding

Thiazide diuretics enter human breast milk in low concentrations. While there are no adequate reports or well-controlled studies in nursing women, they are generally considered compatible with breastfeeding.

Pregnancy

. Chlorotrianisene is an estrogen analog that was and may still be used in some countries for the suppression of lactation. It is ineffective. Chlorotrianisene increases the risk of thromboembolism during

Pregnancy

and postpartum. It is generally considered contraindicated during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in pregnant women. It is unknown whether chlorotrianisene crosses the human placenta. There are suboptimal data linking oral contraceptive use with the VACTERL syndrome.

Breastfeeding

There is no published experience in nursing women. It is unknown whether chlorotrianisene enters human breast milk. 189 The use of estrogen analogs for lactation suppression has been discontinued due to poor efficacy and the risk of thrombosis.

Pregnancy

. There are no adequate reports or well-controlled studies of chlorpheniramine in pregnant women, and its safety during

Pregnancy

is not established. However, it is widely available in OTC preparations and has not to date been implicated in adverse effects during pregnancy. In general, 1st-generation antihistamines are preferred to later generations because of the longer use experience.

Fetal Health

Though there are no adequate reports or well-controlled studies in human fetuses, epidemiologic study suggests chlorpheniramine is not a human teratogen. It is unknown whether chlorpheniramine crosses the human placenta. However, H1 receptors are specifically expressed in syncytiotrophoblast cells of human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. In rodents, chlorpheniramine stimulates glycosaminoglycan alterations leading to palatal mesenchyme and cleft palate malformation.

Breastfeeding

There is no published experience with chlorpheniramine in nursing women. Because preterm and term neonates can have adverse reactions to antihistamines, it should probably be avoided in the 3rd trimester.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Chlorpromazine seems safe and effective when used for the preceding indications during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Chlorpromazine rapidly crosses the placenta, and an extrapyramidal syndrome can occur in newborns of women given chlorpromazine during labor. There is no evidence chlorpromazine is a human teratogen. Rodent studies are also reassuring, though learning and behavioral abnormalities are reported in some studies. The injection of chlorpromazine into each rat uterine horn significantly reduces the number of implantation sites.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Chlorpromazine is excreted into human breast milk, though the kinetics remain to be elucidated. The occasional dose of chlorpromazine is probably compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of chlorpropamide in pregnant women. Current study suggests that some modern oral hypoglycemic drugs are safe and useful, not only later in

Pregnancy

but also in the 1st trimester, providing excellent control of blood glucose. The treatment of women with gestational diabetes after delivery does not appear to alter the timing or reduce the ultimate frequency of type II diabetes. Chlorpropamide and other sulfonylureas may provoke an antabuse-like reaction if the patient consumes alcohol. There are alternative agents with minimal placental transport that are better candidates for maternal therapy. Older reports note its use for diabetes insipidus. Presently, DDAVP is preferred for this indication.

Fetal Health

Chlorpropamide crosses the placenta and has a long t/2. It significantly reduces birth weight and perinatal mortality in the offspring of diabetic women without increasing the incidence of birth defects. More recent studies suggest that some oral hypoglycemic agents are relatively safe during

Pregnancy

with no increased risk of macrosomia, hypoglycemia, and lung 193 immaturity, though there are alternative agents with less placental transfer. Rodent teratogenicity studies have not been conducted.

Breastfeeding

While there are no adequate studies in nursing mothers, chlorpropamide enters the breast milk, achieving an M:P ratio of 0.2, and neonatal hypoglycemia has been reported.

Pregnancy

. Chlorthalidone is an oral diuretic with a prolonged action (48-72h). There are no adequate reports or well-controlled studies in pregnant women. Physiologic edema should not be treated. Thiazide diuretics may be diabetogenic. Severe electrolyte imbalances are reported in both mother and newborn. Hemorrhagic pancreatitis is also reported after thiazide exposure.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Chlorthalidone crosses the placenta, achieving an F:M ratio approximating 0.15. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

While chlorthalidone is excreted into human breast milk, the pharmacokinetics remain to be clarified. It is generally considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Chlorzoxazone should not be taken if there is an allergy to any skeletal muscle relaxant.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether chlorzoxazone crosses the human placenta. Rodent teratogenicity studies have not been performed.

Breastfeeding

There is no published experience in nursing women. It is unknown whether chlorzoxazone enters human breast milk.

Pregnancy

. Cholera vaccine is a sterile suspension of killed V. cholerae. There are no adequate reports or well-controlled studies of cholera vaccine in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is likely cholera vaccine?induced IgG crosses 196 the human placenta. There is no evidence of fetal harm. Rodent studies have not been performed.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Cholera vaccine?induced antibodies enter human breast milk.

Pregnancy

. Cholestyramine is the chloride salt of a basic anion exchange resin that is not systemically absorbed, but could interfere with the uptake of fat-soluble vitamins. Cholestyramine is used by some for the treatment of cholestasis of pregnancy, but its efficacy has long been questioned. The only randomized trial compared it to ursodeoxycholic acid. The results demonstrated cholestyramine was inferior for the relief of prutitus and was associated with worse

Pregnancy

outcomes.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cholestyramine is not systemically absorbed, but could interfere with the uptake of fat-soluble vitamins. Rodent studies are reassuring, revealing no evidence of infertility, increased

Pregnancy

loss, teratogenicity, or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience with cholestyramine in nursing women. The resin is not absorbed from the maternal gut and thus is not secreted into breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies of ciclopirox in pregnant women. Treatment of mycotic cervical inflammation during

Pregnancy

is followed by a significant reduction in symptoms and the number of active colonies.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether ciclopirox crosses the human placenta. Though well absorbed by the pregnant rodent, placental transfer is low, and the fetal tissue concentration is always lower than in maternal blood. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether ciclopirox enters human breast milk.

Pregnancy

. The published experience with cidofovir during

Pregnancy

is limited to a single case report. Its use was associated with breast adenocarcinoma in female rats.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cidofovir crosses the human placenta. However, it was used successfully in a guinea pig model to prevent congenital CMV. Rodent studies conducted at doses below the MRHD revealed maternal toxicity and embryotoxicity associated with skeletal malformations.

Breastfeeding

There is no published experience in nursing women. It is unknown whether cidofovir enters human breast milk. Breastfeeding is contraindicated in HIV-infected nursing women where formula is available to reduce the risk of neonatal transmission.

Pregnancy

. There are no adequate reports or well-controlled studies of cimetidine in pregnant women, and evidence documenting the safety of acid-suppressing drugs during

Pregnancy

is very limited. Antacids and antacid/alginic acid combinations or sucralfate constitute first-line medical therapy. If the symptoms are not adequately relieved or if complications develop, treatment with cimetidine or ranitidine may be considered. The treatment of ??heartburn?? with cimetidine is not followed by significant maternal adverse reactions. Drugs that inhibit hepatic microsomal enzymes, such as cimetidine, may promote the accumulation of unexpectedly high (possibly toxic) blood concentrations of lidocaine. Cimetidine has some antiandrogenic effect.

Fetal Health

There are no adequate reports or well-controlled studies of cimetidine in human fetuses. Studies conducted in pregnant subjects found no relation between drug exposure and birth defects. However, one large epidemiologic investigation noted a possible association between preterm birth and 1sttrimester exposure to H2 antagonists. Further study seems warranted. Rodent studies reveal inhibition of both testicular descent and genital differentiation and postnatal cryptorchidism. These events might occur in human fetuses when high doses of cimetidine are administered to pregnant women around the end of the 1st trimester.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Cimetidine enters human breast milk and is actively transported by BCRP (breast cancer resistance protein). The percentage of the maternal dose ingested based on neonatal body weight is <10%, which should be safe under normal conditions. However, the excretion of alternative agents such as famotidine and nizatidine is even lower.

Pregnancy

. There is no published experience with cinoxacin during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies of cinoxacin in human fetuses. The use of the new quinolones during the 1st trimester of

Pregnancy

is not associated with an increased prevalence of malformations or musculoskeletal problems; however, longer follow-up and MRI of the joints may be warranted to exclude subtle cartilage and bone damage. While rodent studies did not reveal evidence of teratogenicity, cinoxacin was associated with bone development abnormalities in young animals.

Breastfeeding

There is no published experience in nursing women. It is unknown whether cinoxacin enters human breast milk.

Pregnancy

. Fluoroquinolone therapy is widely used as a treatment for gonorrhea because it is a relatively inexpensive, oral, and single- dose therapy. However, fluoroquinolone-resistant disease is being identified more frequently. A test for cure is essential. There are no adequate reports or well-controlled studies in pregnant women. Ciprofloxacin is also usually selected when penicillin- class agents have no effect on gram-negative rods. Ciprofloxacin has the best safety profile of second-line drugs for drug-resistant tuberculosis. It is the drug of choice for prophylaxis among asymptomatic pregnant women exposed to B. anthracis. In instances where the strain is penicillin-sensitive, prophylaxis with amoxicillin, 500mg tid ?60d, may be considered. Isolates of B. anthracis implicated in the recent bioterrorist attacks are susceptible to penicillin in laboratory tests, but may contain penicillinase activity. Penicillins are not recommended for 204 treatment of anthrax. Ciprofloxacin has also been used to treat Q fever during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Ciprofloxacin crosses the human placenta, and can be found in AF in low quantities. The mean transplacental transfer percentage of ciprofloxacin across the isolated perfused human cotyledon approximates 3.2% and the transplacental transfer index (the ratio of transplacental transfer between ciprofloxacin and antipyrine) was 0.34. Short-duration treatment with ciprofloxacin appears free of adverse fetal responses. As a class, the new quinolones do not appear associated with an increased risk of malformation or musculoskeletal problems in humans. The effect of prolonged exposure such as that required for Crohn?s disease or anthrax prophylaxis remains unknown. Longer follow-up and MRI of the joints may be warranted to exclude subtle cartilage and bone damage. There are no clinically significant musculoskeletal dysfunctions reported in children exposed to fluoroquinolones in utero. Treatment of fetal mice, dogs, and rabbits with other quinolones is associated with an acute arthropathy of the weight-bearing joints.

Breastfeeding

There are no adequate reports or well-controlled studies in lactating human mothers. Ciprofloxacin enters human breast milk, and oral doses of this drug are concentrated in breast milk at levels higher than serum. C. difficile pseudomembranous colitis has been reported in a breastfed neonate whose mother was taking ciprofloxacin. In some animals, slow ciprofloxacin elimination results in blood levels out of proportion to that ingested. Though the American Academy of Pediatrics considers it safe for Breastfeeding women, it is probably best to avoid ciprofloxacin when there are reasonable alternatives.

Pregnancy

. There are no adequate reports or well-controlled studies of cisapride in pregnant women. Antacids and antacid/alginic acid combinations or sucralfate constitute first-line medical therapy. 206 Cisapride is reserved for patients with severe symptoms. Rodent studies suggest decreased fertility after exposure to cisapride.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cisapride crosses the human placenta. There were no differences in maternal history, birth weight, gestational age at delivery, and rates of live births, spontaneous or therapeutic abortions, fetal distress, and major or minor malformations among the group of pregnant women exposed to cisapride;3=4 of exposures occurred during organogenesis. Cisapride rapidly crosses the ovine placenta, with an average F:M ratio of 0.71. Embryotoxicity was noted at doses that were multiples of the MRHD. However, a rat study noted the occurrence of a fetal arrhythmia associated with an increased prevalence of malformations.

Breastfeeding

Cisapride enters human breast milk, but at low concentrations of 6ng/ml. Thus, the amount ingested by the neonate is likely without clinical effect.

Pregnancy

. Atracurium is an intermediate-duration curare derivative producing effective surgical paralysis. There are no adequate reports or well-controlled studies of cisatracurium in pregnant women. The clearance and clinical duration of atracurium are unaltered during pregnancy. In contrast, the clearance of pancuronium is increased 27% during cesarean section, and the mean onset time and clinical duration of cisatracurium are significantly reduced.

Fetal Health

There are no adequate reports or well-controlled studies of cisatracurium in human fetuses. Atracurium has been used in lieu of pancuronium to facilitate fetal procedures. While small amounts are shown to cross the human placenta, its use during cesarean section is not associated with neonatal sequelae. In theory, if used for long-term paralysis of a critically ill pregnant woman, fetal toxicity could be a risk. In cell culture, cisatracurium increases the rates of HUVEC apoptosis.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether cisatracurium enters human breast milk. Considering its application, cisatracurium is unlikely to affect the Breastfeeding newborn. While some rodent studies report an increase in malformations, they are confounded by the profound respiratory depression associated with the drug.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Patients should be advised to avoid

Pregnancy

during treatment. The published literature consists mostly of case reports and small series. Good outcomes are possible. Cisplatin has been used during

Pregnancy

for women discovered to have ovarian or other malignancies.

Pregnancy

and fetal age impact on cisplatin protein binding because of lower albumin levels. The resulting higher levels of free drug in the mother and fetus may increase the risk of toxicity in both. Cisplatin causes severe mitochondrial toxicity in the maternal rat kidney. 209

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cisplatin crosses the human placenta. Low fetal protein concentration increases the percentage of free drug. Malformations in offspring of women treated with cisplatin are rare. Cisplatin is embryotoxic and teratogenic in mice. Damage to the fetal renal and hepatic mitochondria as a result of transplacental drug exposure appears mild.

Breastfeeding

Cisplatin enters human breast milk at concentrations at or below the level of detection, and is generally considered compatible with breastfeeding.

Pregnancy

. Depression is an important and often unrecognized problem during

Pregnancy

and the puerperium.

Pregnancy

is not a reason to discontinue therapy.

Pregnancy

increases the metabolism of citalopram necessitating an increasing dose to maintain effect.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Citalopram crosses the human placenta, achieving an F:M ratio approximating 0.66, higher than either sertraline or paroxetine. Several recent epidemiologic studies note an association between 1st trimester SSRI use (most often paroxetine) and CV defects. The concern is great enough the ACOG has suggested caregivers avoid paroxetine in the 1st trimester. The use of antidepressants in early

Pregnancy

does not seem to carry significant risk for the human infant during the newborn period. While the clinical reports are generally reassuring, neonatal withdrawal syndrome has been reported after 3rd trimester exposure. Rodent studies reveal CV and skeletal defects.

Breastfeeding

Citalopram enters human breast milk, but the neonatal concentration is very low and likely poses no threat to Breastfeeding neonates.

Pregnancy

. Clarithromycin is used for the treatment of lower respiratory tract infections, GU tract infections, skin infections, neutropenic patients, AIDS-related infections, acute maxillary sinusitis, and active duodenal ulcer. There are no adequate reports or well- controlled studies in pregnant women. It has been suggested that H. pylori infection might be a cause of persistent hyperemesis gravidarum. Clarithromycin has also been used successfully for the treatment of Q fever, Mediterranean spotted fever and MAC during pregnancy. Studies in rats, rabbits, and monkeys indicate clarithromycin does not impair fertility.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Clarithromycin crosses the human placenta to a greater degree than other macrolides (6% maternal dose), making it a candidate in treatment trials of genital Mycoplasma and Ureaplasma infections during pregnancy. Post-marketing studies are reassuring. No teratogenic effects are noted in most studies of 212 rats, rabbits, and monkeys. However, there are reports of a modest increase in CV malformations and cleft palate in certain rodent strains.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Clarithromycin enters human breast milk, reaching levels as high as 75% of the maternal concentration.

Pregnancy

. See penicillins, amoxicillin, and ticarcillin.

Fetal Health

There are no well-controlled studies in human fetuses. Clavulanate crosses the human placenta, appearing in umbilical blood within 1h after administration, reaching a peak at 2-3h. Rodent studies are reassuring when clavulanate is administered concomitantly with penicillin or amoxicillin, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. 214

Breastfeeding

While there are no reports specifically addressing the passage of clavulanate into the breast milk, it is generally considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies of clemastine during pregnancy. MAOIs such as isocarboxazid, phenelzine, or tranylcypromine prolong the anticholinergic effects of antihistamines. (See chlorpheniramine.)

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether clemastine crosses the human placenta. Symptoms of toxicity in neonates include excitement, hyperreflexia, tremors, ataxia, fever, seizures, fixed dilated pupils, dry mouth, and facial flushing. The dose that causes seizures approximates the lethal dose. (See chlorpheniramine.) 215

Breastfeeding

There is no published experience in nursing women. Clemastine enters breast milk. A 10w old Breastfeeding child developed drowsiness, irritability, refusal to feed, and neck stiffness after maternal use (1mg PO bid); 20h after the last dose, the milk level was 5-10mcg/L and the plasma level 20mcg/L. Caution is advised.

Pregnancy

. Because of its antimicrobial spectrum, clindamycin is used for the treatment of serious infections caused by anaerobes, 216 respiratory tract infections, postpartum endometritis, pneumonitis, and soft tissue infections caused by streptococci and staphylococci. Clindamycin is a popular drug for the treatment of acne in reproductive-age women. Higher doses of clindamycin should be used during pregnancy, as its t/2 in maternal serum appears shorter during pregnancy. When combined with gentamicin in patients with PPROM, there is a significant reduction in the incidence of histologic chorioamnionitis, but not the frequency of funisitis. Oral clindamycin cures BV in 90% and maintains a normal flora in2=3 of treated women throughout pregnancy. The literature is unclear whether clindamycin vaginal gel reduces the incidence of preterm delivery in women with BV?there are randomized trials to support either conclusion. It is the antibiotic of choice for prophylaxis for neonatal group B streptococcal sepsis in patients allergic to penicillin, though there is growing resistance.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Clindamycin crosses the human placenta, achieving fetal levels above the typical MICs. There are no reports linking clindamycin with fetal malformations. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

Clindamycin enters human breast milk. While case reports describe bloody stools in nursing newborns whose mothers were treated with clindamycin, it is usually considered compatible with breastfeeding.

Pregnancy

. Uneven distribution and prolonged retention in the tissues are special features of clofazimine metabolism. There are no adequate reports or well-controlled studies in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Clofazimine crosses the placenta, though the kinetics remain to be elucidated. Hyperpigmentation of the neonate that resolves gradually is reported in humans. Rodent studies are generally reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. However, embryotoxicity and IUGR were noted.

Breastfeeding

Clofazimine is excreted in the breast milk. The average M:P ratio was 1.5, with milk levels of 1.33mg/L and an average infant daily dose of 0.2mg/kg/d. Hyperpigmentation of the newborn resolving over 5mo is reported.

Pregnancy

. There are no adequate reports or well-controlled studies of clofibrate in pregnant women. Clofibrate typically reduces serum cholesterol a modest amount and serum triglycerides somewhat more. Substantial reductions in cholesterol and triglycerides can occur in type III hyperlipidemia. No study has shown a convincing reduction in fatal MI. There is little information on the effect of clofibrate on cholesterol metabolism during human pregnancy. For that reason, women of childbearing potential taking clofibrate should use effective contraception. In patients who plan to become pregnant, clofibrate should be withdrawn several months before conception if deemed medically safe.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether clofibrate crosses the human placenta. It does cross the rodent placenta and alters fetal cholesterol metabolism. While teratogenic studies have not demonstrated any effect attributable to clofibrate, it is known that serum of the rabbit fetus accumulates a higher concentration of clofibrate than that in the mother.

Breastfeeding

There is no published experience in nursing women. It is unknown whether clofibrate enters human breast milk. Animal studies revealed increase in neonatal and pup mortality rates during lactation.

Pregnancy

. There are no indications for clomiphene during pregnancy. Ovarian hyperstimulation may occur even when used as directed. There is an increased incidence of multiple pregnancies, including bilateral tubal

Pregnancy

and coexisting tubal and intrauterine pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether clomiphene crosses the human placenta. Although a myriad of fetal abnormalities are reported in pregnancies after clomiphene-induced ovulation, no discernable pattern has emerged. Rare ocular abnormalities (persistent hyperplastic primary vitreous and retinal aplasia) have been reported in several children of women taking high doses during pregnancy. Rodent studies revealed hydramnios and weak, edematous fetuses with wavy ribs and bone changes.

Breastfeeding

There is no published experience in nursing women. It is unknown whether clomiphene is excreted in human milk. However, clomiphene can inhibit unestablished lactation and should not be used when Breastfeeding is planned.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. A variety of withdrawal symptoms may occur with abrupt discontinuation of clomipramine. Women of reproductive age are frequently prescribed TCAs, and there has been no apparent decline in prescriptions in recent years. The frequent prescription of potentially toxic agents to pregnant women may be due to increases in unplanned pregnancies in industrial countries, lack of adequate scientific evidence on the adverse effects, and conflicting needs to treat maternal diseases and to protect fetuses.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Clomipramine and its major metabolite cross the human placenta, achieving F/M ratios of 0.6 and 0.8, respectively. Withdrawal symptoms, including jitteriness, tremor, and seizures, are reported in neonates whose mothers had taken clomipramine until delivery. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Neonatal clomipramine on days 8-21 produced behavioral and physiologic abnormalities resembling those found in adult human depression.

Breastfeeding

Since only trace amounts of clomipramine are found in human breast milk, it is likely compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. In case reports, clonazepam was unrelated to complications of pregnancy, labor, or delivery. Several investigators have used clonazepam for seizure prophylaxis in severe preeclampsia.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Clonazepam crosses the human placenta, achieving an F:M ratio approximating 0.60. While congenital anomalies are reported in 13% of infants whose mothers took clonazepam during

Pregnancy

in combination with other antiepileptic drugs, there is no pattern of anomalies. The majority 223 of exposed infants are normal at birth and have normal postnatal development. Most series conclude no increase in risk, but all are underpowered to detect an increased prevalence of major malformations. Exposure in the late 3rd trimester and during labor seems to carry greater risks to the perinate. While the neonatal withdrawal syndrome is rare, children born to treated women may have symptoms varying from mild sedation, hypotonia, and reluctance to suck to apnea spells, cyanosis, and impaired metabolic responses to cold stress. These symptoms can persist from hours to months after birth.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing mothers. Clonazepam enters human breast milk. Limited study suggests the Breastfeeding neonate could ingest a clinically relevant amount. Breastfed newborns should be observed closely for

Pregnancy

. Clonidine is popular for treatment-seeking opiate abusers, particularly those with concurrent cocaine use. The abuse potential of the drug warrants further study in this high-risk population. There are no adequate reports or well-controlled studies in pregnant women. Women withdrawing from a variety of illicit narcotics or tobacco may benefit from clonidine initially and then methadone if symptoms persist. The combination of epidural clonidine with bupivacaine/fentanyl for pain control during labor improves analgesia, and reduces the supplementation rate and frequency of shivering. A similar beneficial effect is reported when combined with subarachnoid morphine for post?cesarean section analgesia. Though hypotension and bradycardia are drug dependent, no adverse maternal hemodynamic effects are noted if used in low doses mixed with opioids and local anesthetic. However, troublesome maternal sedation has been reported.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Clonidine readily crosses the placenta, achieving an F:M ratio of 1. Amniotic fluid concentrations are up to 4? those in serum. Neonates of women receiving clonidine during labor are not sedated, but may experience some hypotension. Clonidine does not negatively affect the FHR pattern. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. However, there is an increase in the rate of embryo absorption.

Breastfeeding

Clonidine is concentrated in human breast milk, reaching an M:P ratio approximating 2. Caution is advised.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. All benzodiazepine derivatives are lipophilic, undissociated agents, which readily penetrate membranes. Clorazepate is rapidly absorbed, with peak concentrations 226 reached within 2h. The absorption t/2 approximates 0.77h and the elimination t/2 is 1.3h in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in pregnant women. Clorazepate appears to cross the placenta more slowly than other benzodiazepines (20% compared to 85% for diazepam). An increased risk of malformations is reported in some studies for some benzodiazepines. The lowest effective dose of clorazepate should be used during delivery, because high doses are associated with floppy infant syndrome. Rodent teratogenicity studies apparently have not been performed.

Breastfeeding

Clorazepate is excreted into human breast milk at low concentrations, though the kinetics remain to be detailed. As with other benzodiazepines in breast milk, caution is advised.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Vaginal candidiasis (moniliasis or thrush) is a common and frequently distressing infection for many women. Treatments for 7d may be necessary during

Pregnancy

rather than the shorter courses more commonly used for nonpregnant women. Topical clotrimazole appears to be more effective than nystatin for treating symptomatic vaginal candidiasis in pregnancy. One case-control study concluded women treated with vaginal clotrimazole during

Pregnancy

had a lower prevalence of preterm birth that could not otherwise be explained. There are no trial data to support this observation. Candida sepsis should be considered in the differential diagnosis of sepsis following CVS.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether clotrimazole crosses the human placenta. There is little maternal, systemic absorption after dermal application, and only 3-10% is absorbed after intravaginal administration (<0.03mcg/ml). Thus, considering the dose and route, it is unlikely the maternal systemic concentration will reach a clinically relevant level. One case report describes fetal death at 18w gestation in association with a retained IUD and asymptomatic intra-amniotic and fetal infection by C. albicans. 228 Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing mothers. It is unknown whether clotrimazole enters human breast milk. However, considering the route and level of maternal systemic absorption, it is unlikely the Breastfeeding neonate would ingest a clinically significant amount.

Pregnancy

. Cloxacillin sodium is a broad-spectrum antibiotic effective against penicillinase-producing Staphylococcus and is usually combined with ampicillin. There are no adequate reports or well- controlled studies in pregnant women. Before its withdrawal in 229 the US, cloxacillin was used for the treatment of mastitis. There is a significant increase in the free plasma fraction of cloxacillin during pregnancy, beginning in the 2nd trimester and peaking at delivery. A similarly increased free-of-fraction cloxacillin is found in cord blood, which increases further during the 1st postnatal week. Cloxacillin is highly concentrated in the kidneys.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cloxacillin crosses the human placenta. Fetal drug levels rise slowly to equilibrium within the maternal circulation 1-3h after drug administration. Thereafter, fetal drug levels exceed maternal values. AF levels are low during early gestation, rising progressively near term until they exceed maternal values 6-8h after drug administration. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing mothers. Cloxacillin is excreted in the breast milk of both humans and cows.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Clozapine is a relatively new medication for treatment-resistant schizophrenia. The published experience during

Pregnancy

is limited to case reports. It is effective in responsive patients experiencing positive (hallucinations, delusions, bizarre behavior, hostility) and negative (withdrawal, blunted emotions, lack of motivation, and inability to experience pleasure or enjoyment) symptoms. Negative symptoms seem to respond better to clozapine compared to traditional antipsychotics. Studies in rats revealed a rapid increase in the level of serum prolactin with peak values at 15 and 60min. Clinical experience suggests most current psychotropic drugs are relatively safe for use in pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in the human fetus. It is unknown whether clozapine crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. Clozapine enters human breast milk, achieving an M:P ratio between 2.8 and 4.3 and a milk level of 116ng/ml. It was estimated the nursing infant would ingest <20mcg/kg/d. Animal studies suggest clozapine can affect neonatal behavior. If Breastfeeding continues, the infant should be monitored for possible adverse effects, the drug given at the lowest effective dose, and

Pregnancy

. Cocaine is a highly addictive drug and is abused widely. There are no adequate reports or well-controlled studies in pregnant women. Maternal cocaine use is a significant public health problem, particularly in urban areas and among women of low socioeconomic status. Cocaine stimulates isolated myometrial contractile activity, and several clinical studies report an association between cocaine and preterm labor. Although cocaine inhibits uterine neuronal and extraneuronal uptake of catecholamines, and increases circulating levels of catecholamines in experimental animals, it is unlikely that facilitation of the a-adrenergic pathway is the sole mechanism of action. Cocaine-exposed women have a higher risk of medical complications including syphilis, gonorrhea, and hepatitis; psychiatric, nervous, and emotional disorders; PROM and abruptio placentae; and domestic violence.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing mothers. Cocaine freely enters human breast milk and is stable.

Pregnancy

. Codeine is metabolized to morphine. There are no adequate reports or well-controlled studies in pregnant women. Codeine is contained in many tablets prescribed for the relief of headaches. It is commonly used alone and in combination to relieve episiotomy pain during the puerperium. Combining codeine with an NSAID significantly enhances pain relief. Codeine is not effective for the relief of uterine cramps. Codeine overdose may be reversed with naloxone.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Morphine readily crosses the placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity, though IUGR is seen at doses below those producing maternal toxicity. Neonatal abstinence syndrome is reported.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing mothers. Codeine and its metabolite morphine are excreted in human breast milk. Breastfeeding neonates have low plasma levels during the first few days of life in part secondary to the low concentration in milk, and in part due to the small amount of milk produced. Thus, moderate codeine use (up to 60mg) is probably compatible with breastfeeding.

Pregnancy

. Gout is extremely rare in pregnancy. There are no adequate reports or well-controlled studies in pregnant women. Colchicine is found in some herbs such as Ginkgo biloba. It has been used successfully to treat familial Mediterranean fever. Amniocentesis is typically recommended for women using colchicine at conception. Colchicine-induced myopathy and neuropathy appear more common than previously recognized. Patients receiving long-term therapy should be monitored carefully.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Colchicine crosses the human placenta. While the kinetics remain to be elucidated, it is detectable after maternal ingestion of herbal remedies where the concentration is high enough to affect neutrophil adherence. It does cross the rodent placenta, and is teratogenic at doses of 1.25 and 1.5mg/kg in mice and 10mg/kg in hamsters. Because of its mechanism of action, it is suggested women who take colchicine during fertilization have an increased likelihood of an aneuploid fetus. As a result, some authors do not advise discontinuation of colchicine before

Pregnancy

but recommend amniocentesis for karyotyping. The evidence supporting this recommendation is scant.

Breastfeeding

Colchicine is excreted into human breast milk in low quantities. It usually considered compatible with breastfeeding.

Pregnancy

. There is no published experience with colesevelam during pregnancy. Malabsorption of fat-soluble vitamins might occur during use.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether colesevelam crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in pregnant women. It is unknown whether colesevelam enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Colestipol is an adjunctive therapy for the reduction of elevated serum total and LDL-C in patients with primary hypercholesterolemia (elevated LDL-C) who do not respond adequately to diet. Chronic use of colestipol may lead to increased bleeding secondary to the hypoprothrombinemia of vitamin K deficiency.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether colestipol crosses the human placenta. However, it is not absorbed systemically (<0.17% of the dose), and thus should not directly cause fetal harm at the recommended dosages. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There are no adequate reports or well-controlled studies in Breastfeeding women. Colestipol is not absorbed into the systemic circulation, which suggests a direct effect on

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Cortisone circulates both bound and unbound, the latter active and representing a small percentage. Hepatic synthesis of the steroid-binding protein increases under the influence of estrogen during early pregnancy. Women with Cushing?s disease may require additional cortisone to saturate the newly formed binding protein and prevent the free cortisone level from falling during the first 2 or 3mo of pregnancy. It is suggested but poorly documented that chronic steroid administration increases the incidence of maternal infection. Women who receive a short-term burst of steroids, such as those with PPROM, have no increased incidence of chorioamnionitis. The potent fluorinated steroids, betamethasone and dexamethasone, are more effective at accelerating fetal lung maturity than the less potent corticosteroids, cortisol, cortisone, and prednisone.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Primate studies suggest almost complete conversion of cortisol to cortisone by the placenta. Some suggest emotional stress during organogenesis may cause congenital malformations by increasing the level of cortisone. Retrospective epidemiologic studies have sought an association between oral clefting and exposure to corticosteroids. After controlling for confounding factors, it was concluded that prenatal exposure to corticosteroids increase the risk of cleft lip with or without cleft palate 6-fold. IUGR and shortening of the head and mandible are also suggested sequelae. Yet, the Collaborative Perinatal Project followed women treated during the 1st trimester and, while the number of exposures was limited, no increase in congenital malformations was detected. There was no increase in risk of anomalies after organogenesis. Women exposed to topical 238 cortisone during

Pregnancy

have no significant increase in birth defects. Female rats exposed to cortisone in utero exhibit premature vaginal opening. Cortisone accelerates fetal rat intestinal maturation, perhaps explaining why corticosteroids decrease the incidence of NEC. In sum, the evidence that cortisone is a human teratogen is weak. Cortisone has been reported to reduce short-term variability of the fetal heart rate; a similar phenomenon is recognized with betamethasone.

Breastfeeding

There are no adequate reports or well-controlled studies in Breastfeeding women. Cortisone is present in human milk, but it is unclear whether maternal treatment increases the concentration.

Pregnancy

. Cromolyn is taken daily to prevent symptoms. It is available in an MDI or a nebulizer solution. There are no adequate reports or well-controlled studies in pregnant women. There is an increase in adverse outcomes during

Pregnancy

in women whose asthma is poorly controlled. Intranasal corticosteroids are considered first-line therapy, followed by 1st-generation antihistamines. Rodent studies using parenterally administered drug were not associated with adverse effects.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cromolyn crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically. Adverse fetal effects (increased resorptions and decreased fetal weight) were noted only at very high parenterally administered doses that produced maternal toxicity.

Breastfeeding

There are no adequate reports or well-controlled studies in Breastfeeding women. It is unknown whether cromolyn enters human breast milk. Early prophylaxis against food allergies appears to be best achieved by breastfeeding. Exclusive 240

Pregnancy

. ??Intrinsic factor?? is essential for the adequate alimentary absorption of cyanocobalamin. The recommended daily intake is 4mcg. Cyanocobalamin deficiency and the compensatory rise in homocysteine are significant risk factors for CV disease. There are no adequate reports or well-controlled studies in pregnant women. Cyanocobalamin deficiency has been linked to early

Pregnancy

loss.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. There is efficient transfer of cyanocobalamin against a concentration gradient from mother to fetus by 16w gestation. IUGR fetuses have impaired hepatic cyanocobalamin storage ability. In one study, AF cyanocobalamin levels were lower when the fetus had an NTD. Increased folate intake reduces the risk of NTD and possibly other malformations. Evidence suggests the beneficial effect of folate is related to improved function of methionine synthase, a cyanocobalamin- dependent enzyme converting homocysteine to methionine. Rodent teratogenicity studies have not been performed.

Breastfeeding

While there are no adequate reports or well-controlled studies in Breastfeeding women, cyanocobalamin is generally considered safe for

Pregnancy

. Cyclamate is 30sweeter than sucrose and has been used in foods since the 1950s. It was removed from food products in the US andin the 1970s after several animal studies suggested it posed an increased risk of papillary carcinoma of the bladders in rats fed the maximum dietary level. However, there are no adequate well-controlled studies in human subjects, and epidemiologic study does not suggest an increased incidence of cancer in humans. While still banned in the US, it is available inand Europe. The scientific community is reviewing current data that may support cyclamate approval again.

Breastfeeding

There is no published experience in nursing women. It is unknown whether cyclamate enters human breast milk.

Pregnancy

. Cyclobenzaprine relieves skeletal muscle spasm of local origin without interfering with muscle function. It is ineffective in muscle spasm due to CNS disease. There is no published experience with cyclobenzaprine during pregnancy.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cyclobenzaprine crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically.

Breastfeeding

There is no published experience in nursing women. It is unknown whether cyclobenzaprine enters human breast milk.

Pregnancy

. Cyclophosphamide is an alkylating agent used to treat cancer of the ovary, breast, and blood and lymph systems. Transient sterility is common after cyclophosphamide, and there is a risk of secondary malignancy. There are no adequate reports or well- controlled studies in pregnant women. Multiple case reports suggest it can be used with a good

Pregnancy

outcome, though the loss rate in women with lupus may be increased after 1st trimester administration.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cyclophosphamide crosses the human placenta, though the kinetics remain to be detailed. Population studies have not convincingly demonstrated teratogenicity in humans, though neonatal hematologic suppression and secondary malignancies in the offspring are reported. Studies conducted in rodents suggest an increased incidence of fetal malformations and decreased implantation.

Breastfeeding

Cyclophosphamide enters human breast milk in high concentration and is generally considered not compatible with breastfeeding. Neonatal neutropenia has been reported.

Pregnancy

. There are no adequate reports or well-controlled studies of cycloserine in pregnant women. The published experience is limited to case reports with no obvious pregnancy-related adverse effects.

Breastfeeding

Cycloserine is excreted into human breast milk in small quantities, though the kinetics remain to be detailed. No adverse effects have been reported. It is generally considered compatible with breastfeeding.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Cyclosporine promotes growth of 1st trimester human cytotrophoblasts by apparently increasing their invasive ability. Successful

Pregnancy

after solid organ transplantation is common. Preconception criteria for the optimal transplant recipient include good transplant graft function, no evidence of rejection, a minimum of 1-2y post- transplantation, and either no or well-controlled hypertension. For these women,

Pregnancy

is generally without significant adverse effect. Because preeclampsia develops in 30% of pregnant renal transplant patients, especially those with pretransplantation arterial hypertension, BP, renal function, proteinuria, and weight should be monitored every 2-4w until the 3rd trimester, and then every week. Antihypertensive agents should be changed to those tolerated during pregnancy. Cyclosporine alters placental endothelin-1/NO vasoactive balance, yet newborns of transplant recipient mothers are typically AGA and normotensive.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Transfer of cyclosporine across the isolated perfused placenta is poor, <5% of the maternal load. This is consistent with a case report. Most offspring have normal postnatal growth and development after maternal immunosuppressive therapy. Some studies suggest a higher risk of stillbirth, preterm delivery, and IUGR in transplant patients treated with cyclosporine. Whether this is due to the disease or cyclosporine is unknown. Preliminary evidence suggests prenatal exposure to immunosuppressive drugs does not have a profound effect on the developing immune system. Children born to transplanted women taking cyclosporine have normal renal function despite prolonged exposure in utero.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing mothers. Cyclosporine is excreted into human breast milk at low quantities, though neonatal clearance may be low. In one study, breastfed infants of treated mothers ingested less than 247 300mcg/d and absorbed undetectable amounts. However, in another study of 5 Breastfeeding women, there was a wide range of infant exposures, and 1 infant reached a therapeutic level despite low milk concentrations. In rats, neonatal exposure to cyclosporine in breast milk causes significant alterations in T-cell maturation and inhibition of lymphoproliferative responsiveness to mitogen activation. In rabbits, it reduces the number of nephrons.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. Cyproheptadine is used to prevent or relieve symptoms of rhinitis (inflammation of the mucous membranes of the nasal passages, often associated with hay fever and other seasonal allergies); skin itching and hives; and tissue swelling (angioedema). It is also used to stimulate appetite in women with anorexia nervosa (8mg PO qid).

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether cyproheptadine crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Cyproheptadine alters insulin- secreting beta cell function in the fetal rat pancreas when given to pregnant rats at a dose that has no apparent effects on the maternal pancreas.

Breastfeeding

There is no published experience in nursing women. It is unknown whether cyproheptadine enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. The coexistence of leukemia and

Pregnancy

is extremely rare. Cytarabine is used during

Pregnancy

to achieve remission of the acute episodes. It is an essential component of the drug regimen used for the treatment of AML. Once remission is achieved, the dose should be readjusted.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. Cytarabine does appear to cross the human placenta, though the kinetics remain to be detailed. In humans, cytarabine is associated with fetal brachycephaly, hypoplasia of the anterior cranial base and the midface, cranial synostoses, IUGR, neonatal leukopenia, and elevation of neonatal hepatic transaminases. Unaffected neonates appear to mature normally. In rodents, cytarabine causes microcephalia and joint anomalies.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether cytarabine enters human breast milk.

Pregnancy

. There are no adequate reports or well-controlled studies in pregnant women. There are many case reports of dacarbazine use during

Pregnancy

with a good outcome.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dacarbazine crosses the human placenta. No teratogenic effects are described in human fetuses, and long-term follow-up studies of children exposed in utero in the 1st trimester are reassuring. Dacarbazine is both teratogenic and embryotoxic in rodents when given at multiples of the MRHD.

Breastfeeding

There are no adequate reports or well-controlled studies in nursing women. It is unknown whether dacarbazine enters human breast milk.

Pregnancy

. There is no published experience in pregnant women. It is recommended that women of childbearing potential use contraception before and during therapy, and for 4mo after completion of therapy with daclizumab.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether daclizumab crosses the human placenta. No teratogenic effects are described in human fetuses. Animal teratogenicity studies have not been conducted.

Breastfeeding

There are no published reports in nursing mothers. It is unknown whether daclizumab enters human breast milk.

Pregnancy

. Dactinomycin is a derivative of Streptomyces parvulus and extensively used for the treatment of GTN. No deleterious long- term effects are described in women treated with combination regimens that include dactinomycin for germ cell ovarian cancer. The impact on future fertility appears low. Although remission rates of 80-90% are reported for dactinomycin, women with methotrexate-resistant GTN have a much lower remission rate (60%). Prediction of remission may be more closely related to hCG levels than the WHO score alone. There are no adequate reports or well-controlled studies of dactinomycin in pregnant women.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether dactinomycin crosses the human placenta. No teratogenic effects are described in humans. In rodents, it is both embryotoxic and teratogenic when given at multiples of the MRHD.

Breastfeeding

There is no published experience in nursing women. It is unknown whether dactinomycin enters human breast milk. It is generally considered incompatible with breastfeeding.

Pregnancy

. Dalteparin is a LMWH (5000MW) with improved bioavailability, increased plasma elimination t/2, and greater factor Xa inhibitory activity compared to unfractionated heparin. Dalteparin given once or twice daily (IV or SC) is as effective as unfractionated heparin for the initial treatment of acute DVT. LMWHs are increasingly popular during

Pregnancy

for the treatment of various thrombophilias and the antiphospholipid syndrome, though evidence of their efficacy remains limited. LMWHs differ in pharmacologic profiles. The mean retention time of anti-Xa activity varies from 5.2h (dalteparin) to 7h (enoxaparin, nadroparin). The bioavailability of a prophylactic dose of LMWHs range from 86% (dalteparin) to 98% (enoxaparin, nadroparin). Though equal in efficacy and amenable to once- daily dosing for prophylaxis in the nonpregnant patient, they are more expensive than unfractionated heparin and have the same risks. Heparin and heparin products are not treatments for preeclampsia. However, women with ACE insertion/deletion polymorphism are at increased risk of recurrent disease in a subsequent pregnancy, and 5000IU dalteparin daily reportedly decreases the risk of recurrence. The therapeutic dose of dalteparin during

Pregnancy

is based on maternal weight. Interpatient variability is wide during

Pregnancy

and clearance significantly enhanced. Peak anti-Xa levels occur at 255 4h postbolus in pregnancy, compared with 2h in the nonpregnant state. The mean anti-Xa levels at 12, 24, and 36w gestation are each significantly reduced 2h postinjection, compared with the nonpregnant state. The lowest dose-response curve was at 36w gestation. The initial prophylactic dose for most pregnant women in the 1st trimester is 5000U daily. Anti-Xa activity is measured after initiating therapy, and again periodically (at least each trimester) to confirm the adequacy of the prophylactic or therapeutic dose. A dose of 5000U SC should produce an anti-Xa activity of 0.20-0.40U/ml (0.4-0.7U/ml for full anticoagulation) 3h after injection. Women treated with LMWHs for prevention of thromboembolic complications are at risk of developing an epidural or spinal hematoma after neuraxial anesthesia. It is prudent to wait at least 12h after the removal of an epidural catheter before re-initiating LMWH. LMWHs are best replaced with unfractionated heparin at 36w because of their long t/2s, and inability to rapidly measure residual activity (anti-Xa levels). One prospective study of bone density in women receiving LMWH found no significant change in mean bone density between baseline and 6w postpartum. Another suggested any decrease was consistent with the normal decline associated with pregnancy.

Fetal Health

Dalteparin, similar to other LMWHs and unfractionated heparin, does not cross the placenta. It is generally safe and effective for the noted indications during pregnancy. Rodent studies are reassuring, revealing no evidence of teratogenicity despite the use of doses higher than those used clinically.

Breastfeeding

Only trace amounts of dalteparin (2500U ?1 IU, and measured as anti-Xa activity) enter human breast milk. It is highly unlikely that puerperal treatment would have any clinically relevant effect on the nursing infant.

Pregnancy

. There are no indications during

Pregnancy

for danazol. It should be discontinued if the patient becomes pregnant. Danazol is not 257 an effective contraceptive. It decreases the maternal progesterone level if taken during the 1st trimester.

Fetal Health

There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether danazol crosses the human placenta. Though the FDA classifies danazol as category X, there is no reason a priori to terminate an exposed pregnancy. Danazol can have an androgenic effect on female fetuses (vaginal atresia, clitoral hypertrophy, labial fusion, ambiguous genitalia). Thus, exposed fetuses should undergo a detailed ultrasound examination. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. Danazol is associated with inhibition of fetal development in rabbits.

Breastfeeding

There is no published experience in nursing women. It is unknown whether danazol enters human breast milk. It is generally considered contraindicated during breastfeeding.

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