Aminophylline is a complex of theophylline and ethylenediamine and is given for its theophylline activity to relax smooth muscle and to relieve bronchial spasm. Aminophylline Injection is indicated for relief of bronchospasm associated with asthma and in chronic obstructive pulmonary disease.
Theophylline Derivative; Antiasthmatic/ Bronchodilator
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.
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. INTRAVENOUS Acute severe bronchospasm: Adult: Loading dose: 5 mg/kg (ideal body weight) or 250-500 mg (25 mg/mI) by slow inj or infusion over 20-30 mm. Maintenance infusion dose: 0.5 mg/kg/hr. Max rate: 25 mg/mm. Child: Loading dose: same as adult dose. Maintenance dose: 6 mth-9 yr: 1mg/kg/hr & 10-16 yr: 0.8 mg/kg/hr. EIdery Dose reduction may be ncessary.
Concurrent administration of aminophylline may:
• inhibit the effect of adenosine receptor agonists (adenosine, regadenoson, dipyridamol) and may reduce
their toxicity when used for cardiac perfusion scanning;
• oppose the sedatory effect of benzodiazepines;
• result in the occurrence of arrhythmias with halothane;
• result in thrombocytopenia with lomustine;
• increase urinary lithium clearance.
Therefore these drugs should be used with caution.
Hypersensitivity. Neonates, elderly, lactation, pregnancy, cardiac/hepatic diseases, peptic ulceration. hyperthyroidism, hypertension, epilepsy, heart failure, chronic alcoholism, acute febrile illness.
Nausea, vomiting, abdominal pain, diarrhoea, headache, insomnia, dizziness, anxiety, restlessness; tremor, palpitations. Convulsions, cardiac arrhythmias, hypotension & sudden death after too rapid IV injection.
Not recommended for use during pregnancy and lactation.
Warning: Serious features may develop as long as 12 hours after overdosage with prolonged release
formulations.
Alimentary symptoms: Nausea, vomiting (which is often severe), epigastric pain and haematemesis.
Consider pancreatitis if abdominal pain persists.
Neurological symptoms: Restlessness, hypertonia, exaggerated limb reflexes, convulsions, seizures. Coma
may develop in very severe cases.
Cardiovascular symptoms: Hypotension. Sinus tachycardia is common. Ectopic beats and supraventricular
and ventricular tachycardia may follow.
Metabolic symptoms: Hypokalaemia due to shift of potassium from plasma into cells is common, can
develop rapidly and may be severe. Hyperglycaemia, hypomagnesaemia and metabolic acidosis may also
occur. Rhabdomyolysis may also occur.
Store at temperature not exceeding 30°C in a dry place. Protect from light. Keep out of reach of children.
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