Aminophylline

Indications
Oral
Chronic bronchospasm
Adult: 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.
Hepatic impairment: Dose reduction may be ncessary.
Intravenous
Acute severe bronchospasm
Adult: 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.
Hepatic impairment: Dose reduction may be ncessary.

Special Populations: Reduce maintenance dose in patients with cor pulmonale, heart failure or liver disease and in elderly. Increase maintenance dose for smokers.

Incompatibility: Incompatible with metals.
Contraindications
Hypersensitivity.
Warnings / Precautions
Neonates, elderly, lactation, pregnancy, cardiac/hepatic diseases, peptic ulceration, hyperthyroidism, hypertension, epilepsy, heart failure, chronic alcoholism, acute febrile illness.
Adverse 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.
Overdose Reactions
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.
See Below for More aminophylline Drug Interactions
Food Interactions
Rate of absorption reduced but not extent.
Mechanism of Actions
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.
Absorption: Rate of absorption delayed by food.
Distribution: Crosses the placenta and enters breast milk.
Metabolism: Undergoes hepatic metabolism.
Excretion: Via urine.
Administration
Should be taken on an empty stomach. (Take on an empty stomach at least 1 hr before or 2 hr after meals.)
Storage Conditions
Intravenous: Store below 25°C.
ATC Classification
R03DA05 - aminophylline ; Belongs to the class of xanthines. Used in the systemic treatment of obstructive airway diseases.
Storage
Intravenous: Store below 25°C.
Available As
  • Aminophylline 100 mg
  • Aminophylline 125 mg
  • Aminophylline 200 mg
  • Aminophylline 225 mg
  • Aminophylline 350 mg
  • Aminophylline 72.96 mg
  • Aminophylline 97 mg
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