Antimigren (sumatriptan) coated tablets 50 mg. №1

active ingredient: sumatriptan;

1 tablet contains sumatriptan 50 mg;

excipients: lactose monohydrate, povidone, microcrystalline cellulose calcium croscarmellose sodium stearate; silicon dioxide colloidal titanium dioxide (E 171) hypromellose.

Film-coated tablets.

Basic physical and chemical properties: film-coated tablets, white with a yellowish tint.

Drugs used to treat migraine. Selective serotonin 5HT1 receptor agonists. Sumatriptan. ATX code N02C C01.

Sumatriptan 50 mg is a selective 5HT1 receptor agonist that does not affect other 5HT receptors. These receptors are found mainly in the cranial blood vessels. In experimental studies, it was found that sumatriptan has a selective vasoconstrictive effect on the vessels in the carotid artery system, but does not affect cerebral circulation. The carotid system supplies blood to extra- and intracranial tissues, such as the meninges. Due to the expansion of these vessels, a migraine develops. Additionally, experimental data have shown that sumatriptan inhibits the activity of the trigeminal nerve. These are two possible mechanisms through which sumatriptan antimigraine activity is detected. The clinical effect is observed 30 minutes after taking 100 mg of the drug.

After oral administration, sumatriptan 100 mg. is rapidly absorbed, reaching 70% of the maximum concentration after 45 minutes. After taking 100 mg, the average maximum plasma concentration is 45 ng / ml. Bioavailability after oral administration is 14%, partly due to first pass metabolism, partly as a result of incomplete absorption. Plasma protein binding is low (14-21%), the average volume of distribution is 17 liters. The mean total clearance is approximately 1160 ml/min and the mean renal clearance is approximately 260 ml/min. Non-renal clearance is approximately 80% of total clearance, which suggests that sumatriptan is excreted mainly as metabolites. The main metabolite, the indolocytic analog of sumatriptan, is excreted in the urine, where it is found as a free acid and a glucuronide conjugate. It does not show 5HT1 and 5HT2 activities. Other metabolites have been identified. The pharmacokinetics of oral sumatriptan does not change significantly during a migraine attack.

Antimigraine tablets are prescribed for the rapid relief of migraine attacks, with or without aura. Sumatriptan 50 mg tablets are used only with a clearly established diagnosis of migraine.

Hypersensitivity to the components of the drug.

History of myocardial infarction, ischemic heart disease, Prinzmetal’s angina, peripheral vascular disease, or symptoms consistent with coronary artery disease.

History of stroke or transient cerebrovascular accident.

Moderate or severe hypertension and mild uncontrolled hypertension.

Severe liver failure.

Simultaneous use of ergotamine or its derivatives (including methysergide).

Simultaneous use of any triptan / 5-hydroxytryptamine receptor agonist (5-HT1).

Simultaneous use of monoamine oxidase inhibitors (MAO) and Antimigraine. Antimigraine should not be used within 2 weeks after discontinuation of MAO inhibitors.