AMINOPHYLLINE - Watsons Health

AMINOPHYLLINE

Indications: Listed in Dosage.
Dosage: Adult : PO Chronic bronchospasm As hydrate: Initial: 225-450 mg twice daily, increased if needed.IV Acute severe bronchospasm Loading dose: 5 mg/kg (ideal body wt). Maintenance: 0.5 mg/kg/hr. Rate should not exceed 25 mg/min.
Dosage Details: Intravenous
Acute severe bronchospasmAdult: Loading dose: 5 mg/kg (ideal body weight) or 250-500 mg (25 mg/ml) by slow inj or infusion over 20-30 min. Maintenance infusion dose: 0.5 mg/kg/hr. Max rate: 25 mg/min.
Child: Loading dose: same as adult dose. Maintenance dose: 6 mth-9 yr: 1 mg/kg/hr and 10-16 yr: 0.8 mg/kg/hr.
Elderly: Dose reduction may be ncessary.
Oral
Chronic bronchospasmAdult: As hydrate: Initially, 225-450 mg bid, increased if necessary.
Child: >3 yr: As modified-release hydrate: 12 mg/kg daily increased to 24 mg/kg daily in 2 divided doses after 1 wk.
Elderly: Dose reduction may be ncessary.
Special Patient Group: Reduce maintenance dose in patients with cor pulmonale or heart failure. Increase maintenance dose for smokers.
Hepatic Impairment: Dose reduction may be ncessary.
Administration: Should be taken on an empty stomach. Take at least 1 hr before or 2 hr after meals.
Incompatibility: Incompatible with metals.
Contraindications: Hypersensitivity
Special Precautions: Neonates, elderly, lactation, pregnancy, cardiac/hepatic diseases, peptic ulceration, hyperthyroidism, hypertension, epilepsy, heart failure, chronic alcoholism, acute febrile illness.
Adverse Drug Reactions: Nausea, vomiting, abdominal pain, diarrhoea, headache, insomnia, dizziness, anxiety, restlessness; tremor, palpitations.
Potentially Fatal: Convulsions, cardiac arrhythmias, hypotension and sudden death after too rapid IV injection.
Pregnancy Category (US FDA):

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Overdosage: Symptoms may include agitated maniacal behavior, frequent vomiting, extreme thirst, slight fever, tinnitus, palpitation and arrhythmias. Treatment is usually supportive and withdrawal of the drug. Restoration of fluid and electrolyte balance is necessary.
Drug Interactions: Other xanthines. Clearance reduced by allopurinol, some antiarrhythmics, cimetidine, disulfiram, fluvoxamine, interferon-α, macrolide antibiotics, quinolones, oral contraceptives, thiabendazole and viloxazine. Clearance increased by phenytoin, anticonvulsants, ritonavir, rifampicin, sulfinpyrazone, cigarette smoking. Corticosteroids, diuretics, β2-agonists.
Potentially Fatal: Increased risk of cardiac arrhythmias with sympathomimetics and halothane. Tachycardia with pancuronium. β-blockers inhibit metabolism. Increased risk of convulsion with quinolones, ketamine. 
Food Interaction: Rate of absorption reduced but not extent.
Mechanism of Action: Description: Aminophylline is a combination of theophylline and ethylenediamine. Ethylenediamine is inactive; it increases the solubility of theophylline in water. Theophylline relaxes bronchial smooth muscle. Suggested mechanisms are an increase in intracellular cAMP through inhibition of phosphodiesterase; adenosine receptor antagonism, prostaglandin antagonism and effects on intracellular calcium.
Pharmacokinetics: 
Absorption: Rate of absorption delayed by food.
Distribution: Crosses the placenta and enters breast milk.
Metabolism: Undergoes hepatic metabolism.
Excretion: Via urine.
Storage: Store below 25°C.
Therapeutic Category: Antiasthmatic & COPD Preparations

 

Available Brands:

  • Amilin     
  • Aminosol    
  • Panolin     
  • Phil Pharmawealth/Atlantic Aminophylline
  • Theofil   

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