Zolmitriptan Capsules

Zolmitriptan is a selective 5HTIB/ID receptor agonist. It causes intracranial vasoconstriction and inhibits the release of pro-inflammatory neuropeptides by stimulating 5HTIB/ID receptors on intracranial blood vessels (including arteriovenous anastomoses) and sympathetic nerves of the trigeminal nervous system. Toxicological studies, genotoxicity: In the Ames test, 2 of 5 strains of Salmonella typhi showed mutagenic effects in the presence of metabolic activators. The results of the in vitro mammalian cell mutation test (CHO/HGPRT) were negative. In vivo and in vitro human lymphocyte tests, zolmitriptan showed chromosomal fission effects regardless of the presence of metabolic activators; this effect was not seen in the in vivo micronucleus test in mice. No genotoxicity was shown in the unprogrammed DNA synthesis test. Reproductive toxicity: Male and female rats were given zolmitriptan before mating and during implantation, with a dose of 400 mg/kg/day (the exposure at this dose is about 3000 times that of the maximum recommended human dose of 10 mg/day), and no damage to fertility was shown. In reproductive toxicity studies in rats and rabbits, oral administration of zolmitriptan to pregnant animals resulted in embryolethality and fetal abnormalities. Oral administration of zolmitriptan to pregnant rats during organogenesis at 100, 400, and 1200 mg/kg/day (maternal plasma exposures were approximately 280, 1100, and 5000 times the maximum recommended human daily dose of 10 mg, respectively) resulted in a dose-related increase in embryonic mortality, which was statistically significant at the higher doses. High doses produced maternal toxicity, as evidenced by reduced maternal weight gain during pregnancy. In a similar rabbit study, embryonic mortality was increased at maternally toxic doses of 10 and 30 mg/kg/day (maternal plasma exposures were equivalent to 11 and 42 times the human exposure at the maximum recommended daily dose of 10 mg). At the 30 mg/kg/day dose, an increased incidence of fetal malformations (sternal fusion, rib anomalies) and variations (major vascular variations, irregular rib ossification pattern) was observed. The no-effect dose was 3 mg/kg/day (equivalent to human exposure at the 10 mg dose). When female rats were given zolmitriptan during pregnancy, delivery and lactation, the incidence of hydronephrosis in offspring was found to increase at a maternal toxic dose of 400 mg/kg/day (1,100 times the human exposure). One hour after lactating rats were given zolmitriptan, the drug level in milk was equivalent to the maternal plasma level, and four hours later it was four times the plasma level. Carcinogenicity: A carcinogenicity study of zolmitriptan was conducted on mice and rats at a dose of 400 mg/kg/d administered by oral gavage. The dosing period for female and male mice was 92 weeks and 85 weeks, respectively. The exposure at the highest dose (plasma AUC of the prototype drug) was approximately 800 times that of a single dose of 10 mg (maximum recommended daily dose) in humans. As a result, zolmitriptan had no effect on the incidence of tumors. In the rat experiment, the control, low-dose, and medium-dose groups were dosed for 104 to 105 weeks, and the high-dose group was killed after 101 weeks (male) and 86 weeks (female) due to excessive mortality. As a result, only the 400 mg/kg/day (approximately 3000 times the exposure dose of humans after taking 10 mg) group showed an increase in the incidence of thyroid follicular cell hyperplasia and thyroid follicular cell adenomas in male rats.

The main ingredient of this product is zolmitriptan, and its chemical name is: (S)-4-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl-methyl]-2-oxazolidinone

Indicated for the acute treatment of migraine with or without aura in adults.

The recommended dose for treating migraine attacks is 2.5 mg (one tablet). If symptoms persist or recur within 24 hours, taking the medicine again will still be effective. If a second dose is required, the time should be at least 2 hours apart from the first dose. If the headache is not relieved after taking 2.5 mg (one tablet) of this product, 5 mg (two tablets) can be taken in subsequent attacks. The effect is usually most obvious within 1 hour of taking the medicine. This medicine is equally effective no matter when it is taken during a migraine attack. It is recommended to take it as soon as possible after the onset of the disease. In case of repeated attacks, it is recommended to take no more than 15 mg (six tablets) in a total of 24 hours. This product is not used as a preventive drug for migraine. Patients with renal impairment do not need to adjust the dose when using this product.

The drug is well tolerated. Adverse reactions are mild/mild, transient, and resolve spontaneously without treatment. Possible adverse reactions usually occur 4 hours after taking the drug and do not increase with continued use. The most common adverse reactions include: occasional nausea, dizziness, drowsiness, warmth, weakness, and dry mouth. Paresthesias or sensory disturbances have been reported. Heaviness, tightness, and pressure may occur in the throat, neck, limbs, and chest (with no evidence of ischemic changes on the electrocardiogram), as well as myalgia and muscle weakness.

It is contraindicated for patients who are allergic to any of the ingredients in this product. It should not be used by patients with uncontrolled blood pressure.

Keep in a light-proof and airtight container.

2.5mg

Nanjing Hicin Pharmaceutical Co., Ltd.

• Founded in:

  2003-01-15

• Address:

  No. 1 Hengfa Road, Nanjing Economic and Technological Development Zone

• Tax NO.:

  913201927453675877

• Registered Funds:

  120 million yuan

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