about Mycophenolate class, uses, side effects contraindications
Mycophenolate
Short Description
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.
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.
Trade Name & Company Name
effect of Mycophenolate in Pregnancy, Fetal Health
and Breast feeding
the follwing drugs will increse Mycophenolate by inhepiting cyp450
the follwing drugs will decrease Mycophenolate by inhancing cyp450
trad drugs based on Mycophenolate
| Gen name | Trade name | Catagory name |
| mycophenolate mofetil | CellCept | Selective immunosuppressants |
| Mycophenolate | CELLCEPT 250 MG CAPS | |
| Mycophenolate | CELLCEPT 500MG TAB | |
| Mycophenolate | MOFETAB | |
| Mycophenolate | MYFORTIC 180MG ECTABLET | |
| Mycophenolate | MYFORTIC 360 MG ECTABLET | |
other drugs from same cataogory