Amigren (sumatriptan) capsules 50 mg. N3

active substance: sumatriptan;

1 capsule contains sumatriptan succinate in terms of sumatriptan 50 mg;

excipients: lactose, monohydrate; microcrystalline cellulose; croscarmellose sodium; magnesium stearate;

the composition of the capsule shell: gelatin, titanium dioxide (E 171), Ponceau 4R (E 124).

Capsules.

Main physicochemical properties: hard gelatin capsules No. 1 of cylindrical shape with hemispherical ends; the body is white, the cap is red.

The contents of the capsules are a white or almost white odorless powder.

Selective agonist of 5HT1-receptors of serotonin. Medicines used to treat migraine. ATX code N02C C01.

Sumatriptan is a selective 5HT1-receptor agonist that does not affect other 5HT-receptors. These receptors are found mainly in cranial blood vessels. In the course of research, it was established that sumatriptan exerts a selective vasoconstrictor effect on vessels in the carotid artery system, but does not affect cerebral circulation. The carotid artery system supplies blood to extra- and intracranial tissues, such as the meninges. Due to the expansion of these vessels, a migraine develops. In addition, using experimental data, it was proved that sumatriptan inhibits the activity of the trigeminal nerve. These are two possible mechanisms through which the antimigraine activity of sumatriptan appears.

The clinical effect is observed 30 minutes after oral administration of 100 mg of the drug.

After oral administration, sumatriptan is rapidly absorbed, reaching 70% of the maximum concentration after 45 minutes. After taking 100 mg, the average maximum concentration in blood plasma is 45 ng/ml. Bioavailability after oral administration is 14%, partly due to presystemic metabolism, partly as a result of incomplete absorption. Binding to blood plasma proteins is low (14-21%), the average volume of distribution is 17 l. The mean total plasma 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 in the form of metabolites. The main metabolite, an indole acetate analogue of sumatriptan, is excreted in the urine, where it is found as a free acid and a conjugated compound with a glucuronide. It does not detect 5HT1 and 5HT2 activity. Other metabolites have not been identified. The pharmacokinetics of oral sumatriptan do not change significantly during a migraine attack.

For quick relief of migraine attacks, with or without aura.

• Hypersensitivity to any component of the drug.
• A history of myocardial infarction, coronary heart disease, Prinzmetal’s angina, peripheral vascular disease, or symptoms characteristic of coronary heart disease.
• History of stroke or transient cerebral circulation disorder.
• Moderate or severe arterial hypertension and mild uncontrolled arterial hypertension.
• Severe liver failure.
• Concomitant use of ergotamine or its derivatives (including methysergide).
• Concomitant use of any triptan/5-hydroxytryptamine-receptor (5-HT1) agonist.
• Competitive appointment of monoamine oxidase (MAO) inhibitors and Amigren. Amigren should not be used within 2 weeks after discontinuation of MAO inhibitors.