Zolmitriptan Tablets

Pharmacological action Zolmitriptan is a selective 5-HTIB/ID receptor agonist. It causes intracranial vasoconstriction and inhibits the release of pro-inflammatory neuropeptides by stimulating 5-HTIB/ID receptors on intracranial blood vessels (including arteriovenous anastomoses) and sympathetic nerves of the trigeminal nervous system. It is used to treat migraine with or without aura in adults. Toxicological studies Genotoxicity: In the Ames test, 2 of the 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 a chromosomal fission effect 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 from before mating to implantation at doses up to 400 mg/kg/day (exposure at this dose is approximately 3000 times the maximum recommended human dose of 10 mg/day), and no impairment of fertility was shown. In reproductive toxicity studies in rats and domestic rabbits, oral administration of zolmitriptan to pregnant animals can cause embryonic death and fetal abnormalities. Oral administration of zolmitriptan to pregnant rats during organogenesis at 100, 400 and 1200 mg/kg/day (maternal plasma exposures were 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 high dose. High doses produced maternal toxicity, manifested as reduced maternal weight gain during pregnancy. In a similar domestic rabbit study, embryonic mortality increased at maternally toxic doses of 10 and 30 mg/kg/day (maternal plasma exposures were equivalent to 11 and 42 times the exposure of humans receiving the maximum recommended daily dose of 10 mg). At a dose of 30 mg/kg/day, an increased incidence of fetal malformations (sternal fusion, rib abnormalities) and variations (major vascular variations, irregular rib ossification patterns) was observed. 3 mg/kg/day is a no-effect dose (equivalent to human exposure at a dose of 10 mg). Female rats were given zolmitriptan during pregnancy, delivery, and lactation, and an increased incidence of hydronephrosis in offspring was found at a maternal toxic dose of 400 mg/kg/day (1100 times the human exposure). At 1 hour after administration of zolmitriptan to lactating rats, the drug level in the mammary gland was equivalent to the maternal plasma level, and at 4 hours it was 4 times the plasma level. Carcinogenicity: A carcinogenicity study of zolmitriptan administered orally at a dose of 400 mg/kg/day was conducted in mice and rats. 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 about 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, rats in the control, low-dose, and medium-dose groups were administered for 104 to 105 weeks. The high-dose group was killed after 101 weeks (male) and 86 weeks (female) due to excessive mortality. As a result, only in the 400 mg/kg/day group (about 3000 times the exposure of humans taking 10 mg) did male rats have thyroid follicular cell hyperplasia and an increased incidence of thyroid follicular cell tumors.

White or off-white crystalline powder

This product is a film-coated tablet, which appears white or off-white after removing the coating.

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

(For adults only) One dose is 2.5 mg per tablet. If symptoms persist, a second dose is required 2 hours after the first dose, or if symptoms relapse, the second dose is still effective. The maximum dose within 24 hours should not exceed 15 mg.

Possible side effects include: nausea, dizziness, drowsiness, feeling of warmth, weakness, dry mouth, paresthesia or sensory disturbances. Reports have been made: Feelings of heaviness, tightness and pressure may occur in the throat, neck, limbs and chest, as well as myalgia, muscle weakness, paresthesia and dysesthesia. Most side effects are mild, short-lived and resolve on their own without treatment.

It is contraindicated in children, patients over 65 years old, persons with known hypersensitivity and patients with uncontrolled hypertension.

Precautions for children: The safety and effectiveness of this drug for children have not been determined. Precautions for pregnancy and lactation: There are currently no studies on the use of this drug in pregnant women. This drug should only be considered for use when the benefit to the mother outweighs the potential risk to the fetus. Mammalian studies have shown that zolmitriptan can enter breast milk, but there is no data on human use. Therefore, breastfeeding women should use it with caution. Precautions for the elderly: The safety and effectiveness of this drug for patients over 65 years old have not been determined.

1. There is no evidence that the use of preventive migraine drugs (such as beta-blockers, oral dihydroergotamine, pizotifen) has any effect on the efficacy of this drug. For acute symptomatic treatment, the use of paracetamol, metoclopramide and ergotamine does not affect the pharmacokinetics and tolerability of this product. 2. In healthy individuals, no pharmacokinetic interaction between this product and ergotamine has been observed. The combination of this drug and ergotamine/caffeine is well tolerated, and there is no increase in adverse reactions and no change in blood pressure compared to the use of this drug alone. 3. Avoid the use of other 5HTID agonists within 12 hours of treatment with this drug. After using moxambemide (a specific monoamine oxidase-A inhibitor), the area under the curve of zolmitriptan increased slightly (26%), and the area under the curve of the active metabolite increased slightly (26%).

It should be stored in an environment below 30°C.

2.5mg

24 months

Hainan Haishen Tongzhou Pharmaceutical Co., Ltd.

• Founded in:

  1993-08-03

• Address:

  No. 6, Yaogu 2nd Road, Yaogu Industrial Park, National High-tech Zone, Haikou City, Hainan Province

• Tax NO.:

  91460100283995932K

• Registered Funds:

  10.5 million yuan

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