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|Aminophylline |
Drugs search, click the first letter of a drug name: | A | B | C | D | E | F | G | H | I | J | K | L | M | N | O | P | Q | R | S | T | U | V | W | X | Y | Z | 1 | 2 | 3 | 4 | 5 | 6 | 8 | 9 Home Aminophylline( Theophylline Ethylenediamine ) Pronouncation: (am-in-AHF-ih-lin)Class: Xanthine derivative Trade Names: Trade Names: Trade Names: Trade Names: Phyllocontin-350 (Canada) Mechanism of ActionPharmacologyRelaxes bronchial smooth muscle and pulmonary blood vessels; stimulates central respiratory drive; increases diaphragmatic contractility. PharmacokineticsAbsorption(Note: Information for the pharmacokinetics/dynamics section was taken from theophylline because aminophylline is a mixture of theophylline and base.) Rapidly and completely absorbed in solution or immediate-release. C max is 10 mcg/mL (5 to 15 mcg/mL). T max is 1 to 2 h. Food and antacid does not cause any clinically significant changes; therapeutic range (10 to 20 mcg/mL). Distribution40% protein bound (primarily albumin). Unbound theophylline distributes throughout the body water, but distributes poorly into body fat. Vd is 0.45 L/kg (0.3 to 0.7 L/kg) based on idea body weight. Freely passes across the placenta into breast milk and into CSF. MetabolismDoes not undergo any measurable first-pass elimination. About 90% of dose is metabolized in the liver in adults and children older than 1 yr of age. Caffeine and 3-methylxanthine are the only theophylline metabolites with pharmacological activity. EliminationIn neonates, about 50% of theophylline dose is excreted unchanged in the urine (ie, excretion is by the kidneys). 10% of theophylline dose is excreted unchanged in the urine in children 0 to 3 months of age. Special PopulationsRenal Function ImpairmentNo dosage adjustment required in adults and children over 3 mo. Neonates with reduced renal function, dose reduction and frequent monitoring of serum concentrations are required. Special risk patientsPharmacokinetics vary widely among similar patients and cannot be predicted by age, sex, body weight or other demographic parameters. However, a prolonged t ½ may occur in CHF, liver dysfunction, alcoholism, and respiratory infection patients. Indications and UsagePrevention or treatment of reversible bronchospasm associated with asthma or COPD. Unlabeled UsesTreatment of apnea and bradycardia of prematurity. ContraindicationsHypersensitivity to xanthines (eg, caffeine, theobromine) or ethylenediamine; peptic ulcer; seizure disorders not treated with medication. Aminophylline suppositories are contraindicated in presence of irritation or infection of rectum or lower colon. Dosage and AdministrationDosage is calculated on basis of lean body weight. Oral/RectalDose is determined by percentage of theophylline content in aminophylline salt. Aminophylline is 79% theophylline. Loading Dose Adults and childrenPO/PR 5 mg/kg. Maintenance Dose Healthy nonsmokersPO/PR 3 mg/kg every 8 h. Elderly and patients with cor pulmonale2 mg/kg every 8 h. CHF patients1 to 2 mg/kg every 12 h. Children 9 to 16 yr of age and young adult smokers3 mg/kg every 6 h. Children 1 to 9 yr of age4 mg/kg every 6 h. ParenteralLoading Dose Adults and children not receiving theophylline IV 6 mg/kg. Adults and children receiving theophyllineIV 0.6 to 3.1 mg/kg. Maintenance Dose Healthy nonsmokersIV 0.5 to 0.7 mg/kg/h. Elderly and patients with cor pulmonaleIV 0.3 to 0.6 mg/kg/h. CHF patientsIV 0.1 to 0.5 mg/kg/h. Children 9 to 16 yr of age and young adult smokersIV 0.8 to 1 mg/kg/h. Children 1 to 9 yr of ageIV 1 to 1.2 mg/kg/h. Newborns to infants under 6 moNot recommended. Weigh benefits against risks. Infants 26 to 52 wkDivide into every 6 h dosing. Infants under 26 wkDivide into every 8 h dosing. Infants 6 to 52 wk24 h dosage (mg). Premature infants older than 4 days postnatalIV 1.5 mg/kg every 12 h. Premature infants less than 24 days postnatalIV 1 mg/kg every 12 h. General AdviceIV infusion
Storage/StabilityStore at room temperature. Drug InteractionsAllopurinol, nonselective beta blockers, calcium channel blockers, cimetidine, oral contraceptives, corticosteroids, disulfiram, ephedrine, influenza virus vaccine, interferon, macrolide antibiotics, mexiletine, quinolone antibiotics, thyroid hormonesMay increase aminophylline levels. Aminoglutethimide, barbiturates, hydantoins, ketoconazole, rifampin, smoking (tobacco and marijuana), sulfinpyrazone, sympathomimeticsMay decrease aminophylline levels. Benzodiazepines, propofolAminophylline may antagonize sedative effects. Beta-agonistsEffects of both drugs may be antagonized. Carbamazepine, isoniazid, loop diureticsMay increase or decrease aminophylline levels. FoodSustained-released medications are taken on empty stomach to avoid rapid drug release. Low-protein, high-carbohydrate diet may increase aminophylline levels. Charcoal-broiled foods or high-protein, low-carbohydrate diet may decrease aminophylline levels. HalothaneMay cause catecholamine-induced arrhythmias. KetamineMay result in seizures. LithiumAminophylline may reduce lithium levels. Nondepolarizing muscle relaxantsMay antagonize neuromuscular blockade. IncompatibilityDo not mix with anileridine hydrochloride, ascorbic acid, chlorpromazine, codeine phosphate, dimenhydrinate, dobutamine hydroxide, epinephrine, erythromycin gluceptate, hydralazine, insulin, levorphanol tartrate, meperidine, methadone, methicillin, morphine sulfate, norepinephrine bitartrate, oxytetracycline, penicillin G potassium, phenobarbital, phenytoin, prochlorperazine, promazine, promethazine, tetracycline, vancomycin, verapamil, vitamin B complex with vitamin C. Laboratory Test InteractionsNone well documented. Adverse ReactionsCardiovascularPalpitations; tachycardia; hypotension; arrhythmias. CNSIrritability; headache; insomnia; muscle twitching; seizures. GINausea; vomiting; anorexia, diarrhea; gastroesophageal reflux; epigastric pain. GenitourinaryProteinuria; diuresis. RespiratoryTachypnea; respiratory arrest. MiscellaneousFever; flushing; hyperglycemia; inappropriate antidiuretic hormone secretion; sensitivity reactions (exfoliative dermatitis and urticaria). Precautions
PregnancyCategory C . LactationExcreted in breast milk. ChildrenSafety and efficacy not established in children under 1 yr of age. Cardiac effectsAminophylline may cause or worsen preexisting arrhythmias. GI effectsAminophylline may cause or worsen preexisting ulcers or gastroesophageal reflux. Status asthmaticusIn this medical emergency parenteral medication and close monitoring in intensive care unit are recommended. ToxicityPatients with liver impairment or cardiac failure and those more than 55 yr of age are at greatest risk. Patient Information
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