about Aminophylline class, uses, side effects contraindications
Aminophylline
Short Description
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.
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.
Trade Name & Company Name
effect of Aminophylline in Pregnancy, Fetal Health
and Breast feeding
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.
the follwing drugs will increse Aminophylline by inhepiting cyp450
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the follwing drugs will decrease Aminophylline by inhancing cyp450
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trad drugs based on Aminophylline
| Gen name | Trade name | Catagory name |
| aminophylline | Phyllocontin | Methylxanthines |
| Aminophylline | AMINOPHYLLINE 250 Mg INJECTION | |
| Aminophylline | AMINOPHYLLINE INJ 250MG | |
| Aminophylline | NEOPHYLLIN TAB 100MG | |
other drugs from same cataogory