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International generic name
Aminophylline
Drug form and composition
Solution for injection. One ampoule of 10 ml (2.4 %) contains 240 mg Aminophylline
(24 mg/ml).
Indications
Acute attacks of bronchial asthma or spastic bronchitis; bronchial spasm in acute
and exacerbated chronic obstructive pulmonary diseases; neonatal apnea as a respiration
stimulator; in overdosage or intoxication with dipyridamol as a counter-poison.
Dosage and administration
Usual dose in adults is 240-480 mg, diluted in solvent in ratio 25 mg Sophafyllin
per ml solvent. The solution is injected very slowly intravenously (within 20 minutes).
As an intravenous infusion the preparation is used in a single dose of 5 mg per
kg body weight within 20-30 minutes. In children usual single dose is 5-10 mg/kg,
applied intravenously (within 20-30 minutes). Maintaining dose in children aged
from 6 months to 9 years is 1 mg per kg body weight per hour, whereas in children
aged 10-16 years it is 0.8 mg per kg body weight per hour.
Contraindications
Hypersensitivity to the preparation; acute pulmonary edema; congestive heart
failure; tachyarrhythmias; severe liver diseases; active ulcer disease; acute gastritis;
gastro-esophageal reflux; hypothyroidism; convulsive diseases; sepsis.
Special warnings and precautions
In patients with congestive heart failure, liver failure, overweight, cor pulmonale,
and elderly persons the preparation should be used with care. On smokers higher
doses should be used, as the Sophafyllin half-life in such patients is shorter,
compared to nonsmokers. Intramuscularly application of the preparation is not advisable,
due to the slow absorbtion and local pain in the place of application. In pregnant
and nursing women administration of Sophafyllin is not advisable.
Drug interactions
The plasma level of Sophafyllin is elevated in concomitant application of cimetidin,
erythromycin, alopurinol, and oral contraceptives. In simultaneous treatment with
enzyme inductors (phenobarbital, carbamazepine, phenytoin, rifampicin) clearance
of Sophafyllin is increased, which requires an enhancement of the dose. Sophafyllin
increases the lithium preparation excretion. In concomitant treatment with propranolol
it antagonizes the effect of the latter. Sophafyllin potentiates the action of furosemide
and side effects of adrenergic drugs.
Adverse reactions
The preparation may provoke following adverse reactions: tachycardia, hypotension,
precordial pain; cardiac rhythm disorders and orthostatic collapse (rarely); dizziness;
headache; insomnia; paresthesias; convulsions; nausea; vomiting; urticaria.
Pharmacological mechanisms
Sophafyllin exerts a direct myotropic effect on the smooth muscles of the blood
vessels and bronchi, due to an inhibition of enzyme phosphodiesterase in the cells.
Clinically this effect is manifested by a fast and powerful bronchodilation and
dilation of the peripheral and coronary blood vessels. Sophafyllin improves the
brain circulation also, which leads to reduction of the intracranial pressure in
stroke. It exerts a positive inotropic effect on the heart muscle, increasing the
oxygen consumption of the myocardium. The preparation increases glomerular filtration
in the kidney, as well as the diuresis. It exerts some antihistamine and desensitization
actions.
Supplied
50 ampoules of 10 ml (240 mg).
Expiry
3 years.
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