Product Information:
| Product name |
Aminophylline Tablets |
| Specifications |
100mg |
| Package |
10 * 10/Box |
| Storage |
Cool & Dry Place |
| Quality standard |
BP. |
| Shelf Life |
3 Years |
Indication:
It is suitable for relieving asthma, asthmatic bronchitis, obstructive emphysema, etc. it can also be used for asthma caused by cardiogenic pulmonary edema.
Pharmacology and Toxicology:
This product is theophylline and ethylenediamine double salt, its pharmacological action mainly comes from theophylline, ethylenediamine enhances its water solubility. This product has direct relaxation effect on airway smooth muscle. In the past, it was thought that the inhibition of phosphodiesterase resulted in the increase of cAMP content in cells. Recent studies suggest that theophylline's bronchiectasis is partly due to the release of endogenous epinephrine and norepinephrine. In addition, theophylline is a purine receptor blocker, which can resist the contractile effect of adenine on respiratory tract. Theophylline can enhance the contractility of diaphragm, especially when the diaphragm is weak, so it is beneficial to improve the respiratory function.
Pharmacokinetics:
Oral administration of this product can be quickly absorbed. Theophylline was released from aminophylline in vivo, and the protein binding rate of the latter was 60%. T1 / 2: newborns (within 6 months) > 24 hours, children (more than 6 months) 3.7 hours ± 1.1 hours, adults (non-smokers without asthma) 8.7 hours ± 2.2 hours, smokers (1-2 packs a day) 4-5 hours.
The plasma concentration of the drug reached the peak within 2 hours after oral administration on an empty stomach. Most of the products are excreted through the kidney in the form of metabolites, and 10% are excreted in the original form.
Adverse reactions:
The toxicity of theophylline often appears in the serum concentration of 15-20 μ g / ml, especially at the beginning of treatment. Nausea, vomiting, irritability, insomnia and so on are common in the early stage. When the serum concentration exceeds 20 μ g / ml, tachycardia and arrhythmia can occur. When the serum concentration of theophylline exceeds 40 μ g / ml, fever, dehydration, convulsion and other symptoms can occur, and even respiratory and cardiac arrest can cause death.
Matters needing attention:
1. This product is not suitable for patients with persistent asthma or acute bronchospasm attack;
2. The serum theophylline concentration should be monitored regularly to ensure the maximum curative effect without the risk of high blood concentration;
3. Patients with renal or liver dysfunction, aged over 55 years old, especially male patients with chronic lung disease, heart failure caused by any reason, and persistent fever. The maintenance time of serum theophylline concentration is often significantly prolonged in patients who use some drugs or whose theophylline clearance rate is decreased after discontinuing the combination of drugs. The dosage should be adjusted or the interval should be prolonged;
4. Theophylline can cause arrhythmia and / or worsen the original arrhythmia; any change of heart rate and / or rhythm should be monitored and studied;
5. Patients with hypoxemia, hypertension or peptic ulcer history should use this product with caution;
6. This product can pass through the placental barrier and secrete into the milk. It can be discharged with the milk. Pregnant women, puerpera and lactating women should use it with caution;
7. Neonatal plasma clearance rate can be reduced and serum concentration increased, so it should be used with caution;
8. Due to the decrease of plasma clearance rate and the increase of potential toxicity in the elderly, 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 and increase the blood concentration and toxicity of the drug when combined with the drug.
2. Cimetidine can reduce the liver clearance rate of the product, and increase the serum concentration and / or toxicity of theophylline when combined.
3. Some antibiotics, such as erythromycin, roxithromycin, clarithromycin, enoxacin, ciprofloxacin, ofloxacin, levofloxacin, clindamycin and lincomycin, can reduce the clearance rate of theophylline and increase its plasma concentration, especially erythromycin and enoxacin. When theophylline is combined with the above drugs, it should be reduced appropriately.
4. Phenobarbital, phenytoin and rifampicin can induce hepatic drug enzymes and speed up the liver clearance rate of theophylline; theophylline also interferes with the absorption of phenytoin, and the plasma concentration of phenytoin and phenytoin decreases, so the dosage should be adjusted when they are used together.
5. When combined with lithium salt, the renal excretion of lithium increased. It affects the function of lithium salt.
6. In combination with mexiletine, it can reduce the clearance rate of theophylline and increase the concentration of theophylline in plasma.
7. When used together with caffeine or other xanthine drugs, its effect and toxicity can be increased.
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