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Aminophylline Tablets

Function and Efficacy

This product is a complex salt of theophylline and ethylenediamine. Its pharmacological effect mainly comes from theophylline, and ethylenediamine increases its water solubility. This product has a direct relaxant effect on respiratory smooth muscle. Its mechanism of action is relatively complex. In the past, it was believed that it was caused by inhibiting phosphodiesterase and increasing the intracellular cAMP content. Recent experiments have shown that the bronchodilator effect of theophylline is partly due to the release of endogenous adrenaline and norepinephrine. In addition, theophylline is a purine receptor blocker that can counteract the contractile effect of adenine and other substances on the respiratory tract. Theophylline can enhance the contraction of the diaphragm, especially when the diaphragm contraction is weak, so it is beneficial to improve respiratory function.

Ingredients

This product mainly contains aminophylline, and its chemical name is 1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione-1,2-ethylenediamine salt dihydrate. Molecular formula: C2H8N2 (C7H8N4O2)2·2H2O Molecular weight: 456.46

Name Description Content CAS NO. Manufacturer
AminophyllineIngredients

It has a direct relaxant effect on the smooth muscles of the respiratory tract. Its mechanism of action includes inhibiting phosphodiesterase, increasing the intracellular cAMP content; partially achieving bronchial dilation by releasing endogenous adrenaline and noradrenaline; acting as a purine receptor blocker to counteract the contractile effect of adenine on the respiratory tract; and enhancing the contractility of the diaphragm and improving respiratory function.

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317-34-0 10

Appearance

This product is white or slightly yellow tablets.

Indication

This medicine is suitable for relieving wheezing symptoms of bronchial asthma, asthmatic bronchitis, obstructive pulmonary emphysema, etc.; it can also be used for asthma caused by cardiogenic pulmonary edema.

Usage and Dosage

1Usually used oral dose for adults: 0.1-0.2g at a time, 0.3-0.6g per day; Maximum dose: 0.5g at a time, 1g per day. 2Usually used oral dose for children: 3-5mg/kg per time, 3 times a day.

Adverse Reactions

The toxicity of theophylline often occurs at a serum concentration of 15-20μg/ml, especially at the beginning of treatment. Common symptoms in the early stage include nausea, vomiting, irritability, insomnia, etc. When the serum concentration exceeds 20μg/ml, tachycardia and arrhythmia may occur. When the theophylline in the serum exceeds 40μg/ml, symptoms such as fever, dehydration, and convulsions may occur. In severe cases, respiratory and cardiac arrest may occur, leading to death.

Precautions

It is contraindicated for patients who are allergic to this product, those with active peptic ulcers and uncontrolled convulsive diseases.

Special Population Medication

Precautions for children: The plasma clearance rate of newborns may be reduced and the serum concentration may increase, so it should be used with caution. Precautions for pregnancy and lactation: This product can pass through the placental barrier and can also be secreted into breast milk and excreted with breast milk. It should be used with caution by pregnant women, parturients and lactating women. Precautions for the elderly: The plasma clearance rate of the elderly is reduced and the potential toxicity is increased. It should be used with caution in patients over 55 years old.

Drug Interactions

1. Diltiazem and verapamil can interfere with the metabolism of theophylline in the liver. When used in combination with this product, the blood concentration and toxicity of this product will be increased. 2. Cimetidine can reduce the liver clearance rate of this product. When used in combination, it can increase the serum concentration and (or) toxicity of theophylline. 3. Certain antibacterial drugs, such as erythromycin, roxithromycin, clarithromycin of macrolides, enoxacin, ciprofloxacin, ofloxacin, levofloxacin, clindamycin, lincomycin of fluoroquinolones, etc., can reduce the clearance rate of theophylline and increase its blood concentration, especially erythromycin and enoxacin. When theophylline is used in combination with the above drugs, the dosage should be appropriately reduced. 4. Phenobarbital, phenytoin, and rifampicin can induce liver enzymes and accelerate the liver clearance rate of theophylline; theophylline also interferes with the absorption of phenytoin. The plasma concentrations of both are reduced. The dosage should be adjusted when used in combination. 5. When used in combination with lithium salts, the renal excretion of lithium can be increased. Affect the effect of lithium salts. 6. When used in combination with mexiletine, the clearance of theophylline can be reduced, the concentration of theophylline in plasma can be increased, and the dosage needs to be adjusted. 7. When used in combination with caffeine or other xanthine drugs, their effects and toxicity can be increased.

Storage

Keep away from light and store in a sealed container.

Packaging Specification

0.1 g

Validity Period

18 months

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