What are the effects of aminophylline?

Many people have poor gastrointestinal function and are often plagued by viruses and bacteria, which seriously affect gastrointestinal metabolism. Some patients also suffer from long-term asthma, wheezing, cardiopulmonary failure, and heart disease. These symptoms can be treated and relieved using aminophylline. Aminophylline is a Western medicine clinically and has certain environmental effects on all aspects of the body. However, the right medicine must be prescribed before use to avoid side effects or complications caused by incorrect or inappropriate methods.

This product is the double salt of theophylline and ethylenediamine

Its pharmacological effect mainly comes from theophylline, and ethylenediamine enhances its water solubility. Insoluble in methanol, ethanol and ether. This product has a direct relaxant effect on respiratory smooth muscles. Its mechanism of action is relatively complex. In the past, it was believed that it increased the intracellular cAMP content by inhibiting phosphodiesterase. Recent experiments suggest that the bronchodilator effect of thea alkaloids is partly due to the release of endogenous adrenaline and norepinephrine. In addition, thea alkaloids are purine receptor blockers that can counteract the contractile effects of adenine and other substances on the respiratory tract. Theacrine can enhance the contraction force of the diaphragm, especially when the diaphragm contraction is weak, so it is beneficial to improve respiratory function. This product also has a slight effect of relaxing the smooth muscles of coronary arteries, peripheral blood vessels and bile ducts. It has a slight increase in contractility and a slight diuretic effect.

Pharmacodynamics

It is a complex salt of theophylline and diethylamine. Its pharmacological effect mainly comes from theophylline, and ethylenediamine enhances its water solubility. ① It can relax bronchial smooth muscles, as well as various smooth muscles such as the intestines and bile ducts, and can also relieve congestion and edema of the bronchial mucosa. ② Increase cardiac output, dilate the output and input renal arterioles, increase glomerular filtration rate and renal blood flow, and inhibit the reabsorption of sodium and chloride ions in the distal renal tubules. ③ Increase the contractility of isolated skeletal muscle; improve muscle contractility in cases of chronic obstructive pulmonary disease. The increase in hypoxic ventilatory insufficiency caused by theacrine is thought to be due to its increased diaphragmatic contraction, which in turn has an effect beyond that of the respiratory center.

Pharmacokinetics

This product can be rapidly absorbed by oral administration, rectal administration or parenteral administration. In the body, aminophylline releases theaphylline, the latter of which has a protein binding rate of 60%. The volume of distribution (Vd) is approximately 0.5L/kg. The half-life is 3 to 9 hours. If 6 mg/kg of aminophylline is injected intravenously within half an hour, its blood concentration can reach 10 mg/L. Its bioconversion rate in the body varies among individuals. When this product is taken orally on an empty stomach, the blood concentration reaches its peak within 2 hours. Most of this product is excreted through the kidneys in the form of metabolites, and 10% is excreted in its original form.

Indications

It is suitable for relieving wheezing symptoms of bronchial asthma, asthmatic bronchitis, obstructive pulmonary emphysema, etc.; it can also be used for asthma caused by heart failure (cardiogenic asthma).