Why do children use dipyridamole?

The life expectancy of ancient people was much shorter than ours today. The improvement in living standards and medical care are the reasons why people's life expectancy has been extended. Health issues are issues that we have always been concerned about, and children's health is especially our focus. After all, if the youth are strong, China will be strong. Some children take dipyridamole because of illness. What is the effect of dipyridamole?

Dipyridamole (Chinese Pharmacopoeia name: Dipyridamole, trade name Persantine) is a drug that dilates coronary arteries and prevents thrombosis. It is mainly used for ischemic heart disease and stroke, and is also used in small quantities to treat other diseases.

Side effects may include headache, dizziness, nausea, vomiting, diarrhea, etc.; combined use with heparin may cause bleeding tendency; occasional rash, coronary artery steal phenomenon

. There are three main types of drugs: dipyridamole injection, dipyridamole sustained-release capsules and dipyridamole tablets. It was a commonly used drug for the treatment of coronary heart disease in the early years, but is now rarely used to prevent myocardial ischemia. Its antiplatelet aggregation effect can be used in heart surgery or valve replacement to reduce the formation of thromboembolism.

Pharmacology and Toxicology

It has anti-thrombotic effect. Dipyridamole inhibits platelet aggregation, and high concentrations (50 μg/ml) can inhibit platelet release.

The mechanism of action may be:

⑴ Inhibit platelet uptake of adenosine, which is a platelet response inhibitor;

⑵Inhibit phosphodiesterase, increasing cyclic adenosine monophosphate (cAMP) in platelets;

⑶Inhibits the formation of thromboxane A2 (TXA2), a strong agonist of TXA2 platelet activity;

⑷ Enhance endogenous PGI2.

Dipyridamole has a vasodilatory effect. Intraduodenal administration of dipyridamole 0.5-4.0 mg/kg to dogs produced dose-related decreases in systemic and coronary vascular resistance, decreases in systemic blood pressure, and increases in coronary blood flow. The drug takes effect 24 minutes after administration and lasts for about 3 hours. The same hemodynamic effects are observed in humans. However, acute intravenous administration can reduce local myocardial perfusion in the distal part of the stenotic coronary artery. In 111-week oral studies in mice and 128-142 weeks in rats, dipyridamole at doses of 8, 25, and 75 mg/kg (1, 3.1, and 9.4 times the maximum recommended daily dose for humans) did not produce significant carcinogenic effects. The results of the mutagenicity test were negative. Reproduction studies in rats using 60 times the maximum recommended human daily dose of dipyridamole showed no evidence of reproductive impairment. However, at 115 times the maximum recommended daily dose for humans, the number of corpora lutea was significantly reduced and live embryo implantation decreased. Studies in mice, rats, and rabbits showed no evidence that dipyridamole harmed the fetus. The oral LD50 for mice is 2150 mg/kg; the single oral lethal dose is 6000 mg/kg in rats and 350 mg/kg in dogs.

Pharmacokinetics

Dipyridamole injection: plasma half-life is 2 to 3 hours. Highly bound to plasma proteins. It is metabolized in the liver, conjugated with glucuronic acid, and excreted in the bile.

Dipyridamole sustained-release capsules: After oral administration, the peak plasma concentration takes about 2 hours to reach, the steady-state peak plasma concentration is 1.98 μg/ml (1.01~3.99 μg/ml), the steady-state trough concentration is 0.53 μg/ml (0.18~1.01 μg/ml), the plasma protein binding rate is 99%, and the half-life is about 12 hours. It is metabolized in the liver and excreted in the bile after conjugation with glucuronide.

Dosage

Dipyridamole injection: 0.142 mg/(kg·min), intravenous drip for 4 minutes.

Dipyridamole sustained-release capsules: 200 mg orally, twice a day.

Dipyridamole tablets: Oral. Take 25-50 mg at a time, 3 times a day, before meals. Or follow doctor's advice.

Precautions

⑴ It can cause peripheral vasodilation, so it should be used with caution in patients with hypotension.

⑵ It should not be mixed with other drugs other than glucose for injection.

⑶ Combination with heparin may cause bleeding tendency.

⑷ Use with caution in patients with bleeding tendency.

Use in pregnant and lactating women: No appropriate controlled studies have been conducted in pregnant women and this drug should only be used in pregnant women when necessary. Dipyridamole is excreted in human breast milk and should be used with caution in lactating women.

Use in children: The safety and effectiveness of this drug for children under 12 years of age have not been established.