Aminophylline is a compound of the bronchodilator theophylline with ethylenediamin in 2:1 ratio. Aminophylline is less potent and shorter-acting than theophylline. Its most common use is in the treatment of airway obstruction from asthma or COPD.

Aminophylline is a compound salt of theophylline and ethylenediamine, which belongs to xanthine class of drugs, and its pharmacological effects are mainly derived from theophylline, which has the strongest relaxing effect on airway smooth muscle among the xanthine class of alkaloids, and its water solubility can be enhanced by ethylenediamine.

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Aminophylline is suitable for the treatment of bronchial asthma, obstructive emphysema and wheezing bronchitis, not only can relax the bronchial smooth muscle, 

but also cardiotonic, diuretic, coronary dilation, anti-inflammatory, antagonistic adenosine receptors, immune regulation, 

excitation of the respiratory center, etc., and thus can be used in the treatment of asphyxia of preterm infants, sick sinus syndrome, acute lung injury and other diseases.

Aminophyllinum is a commonly used bronchodilator, can directly relax the bronchial tubes and bile ducts and other smooth muscles to relieve spasm.

 Indirectly inhibit the release of histamine and other allergic substances; and can enhance myocardial contractility, increase cardiac output, 

and can have vasodilator effect on coronary arteries, but generally not used as an anti-angina drug.

It has good diuretic effect. Its effective concentration is 10-15mg/L, more than 20mg/L can cause poisoning. Aminophylline can be poisoned by a 

large dose or short-term frequent use of the drug, in addition to intravenous administration of too high a concentration or too fast can lead to poisoning.

Pharmacological effect

1. Relaxation of airway smooth muscle: Aminophylline can relax airway smooth muscle and relieve bronchial spasm.

2. Immunomodulation and anti-inflammatory effects: small amount of aminophylline can inhibit mast cells to release inflammatory transmitters, relieve airway smooth muscle spasm; also can inhibit bronchial eosinophil infiltration.

3. Enhance the contractility of respiratory muscle: preventing and controlling diaphragm fatigue and respiratory failure by improving respiratory function.

4. Excitement of respiratory center: make respiration excited, enhance the depth of respiration, but the respiratory frequency does not increase.

5. Cardiotonic: acts on heart, antagonizes adenosine, prevents excessive release of adenosine, dilates coronary artery and peripheral blood vessels, promotes myocardial contraction, and increases cardiac output.

6. Diuretic: increase renal blood flow and glomerular filtration rate, inhibit tubular reabsorption.

Drug interaction

1. Verapamil may interfere with the metabolism of theophylline in the liver, and when combined may increase the blood concentration and toxicity of this product.

2. Cimetidine can reduce the hepatic clearance of this product, and can increase serum concentration or toxicity when used in combination.

3. Certain antibacterial drugs, such as macrolides erythromycin, erythromycin, clarithromycin, fluoroquinolones enoxacin, ciprofloxacin, oxfloxacin, levofloxacin, as well as clindamycin, lincomycin, etc., can reduce theophylline clearance, increase its blood concentration, especially erythromycin and enoxacin, when theophylline and the above drugs used together, the amount should be reduced appropriately.

4. Phenobarbital, phenytoin sodium, rifampicin can induce hepatic enzymes, accelerate the hepatic clearance of theophylline; theophylline also interferes with the absorption of phenytoin sodium, both plasma concentrations are decreased, the dose should be adjusted when used together.

5. Combined with lithium salts, can increase the renal excretion of lithium; affect the effect of lithium salts.

6. Combined with mexiletine, can reduce the clearance of theophylline, increase the plasma concentration of theophylline, need to adjust the dose.

7. Combining with caffeine or other xanthines may increase their effects and toxicity.

8. Magnesium sulfate can antagonize the arrhythmia caused by this product.

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