Drug name

Imitrex (Sumatriptan)

Pharmacological action

Imitrex (Sumatriptan) is a specific selective agonist of 5-NT1-serotonin receptors, localized mainly in blood vessels of the brain and their stimulation leads to narrowing of these vessels. Does not affect other subtypes of 5-NT-serotonin receptors (5-NT2-7). Activates the sensitivity of trigeminal nerve receptors. The therapeutic effect usually occurs 30 min after administration.

Pharmacokinetics

After oral administration, it is rapidly absorbed. 70% of maximum plasma concentration is reached after 45 min. Cmax in blood plasma is 54 ng/ml. Bioavailability is 14% (due to presystemic metabolism and incomplete absorption). Binding to plasma proteins is 14-21%.

Metabolized by oxidation with the participation of monoamine oxylase (mainly isoenzyme A) to form metabolites, the main of which are indole acetic analog of sumatriptan, which has no pharmacological activity against 5-HT1-serotonin receptors, and its glucuronide. It is excreted by the kidneys, mainly as metabolites.

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Contraindications to use

• Hemiplegic, basilar or ophthalmoplegic forms of migraine;
• CHD or presence of symptoms suggestive of it;
• history of myocardial infarction;
• pharmacologically uncontrolled arterial hypertension;
• peripheral vascular occlusive disease;
• stroke or transient cerebral circulation disorder (including history);
• Severe hepatic or renal dysfunction;
• concomitant use with ergotamine or its derivatives and within 24 hours after their administration;
• use while taking MAO inhibitors or earlier than 2 weeks after withdrawal of these drugs;
• Under 18 and over 65 years of age (efficacy and safety have not been established);
• pregnancy;
• breastfeeding (breastfeeding is possible not earlier than 24 hours after taking the drug;
• congenital galactosemia, glucose/galactose malabsorption syndrome, congenital lactose deficiency;
• hypersensitivity to any of the ingredients of the drug.

Caution: epilepsy (including any condition with reduced epileptic threshold), pharmacologically controlled arterial hypertension, hepatic or renal dysfunction, hypersensitivity to sulfonamides (administration of sumatriptan may cause allergic reactions, intensity of which varies from skin manifestations to anaphylaxis).

Administration during pregnancy and lactation

Contraindicated during pregnancy and breast-feeding (breast-feeding possible not earlier than 24 hours after taking the drug).

Indications of the drug Imitrex (Sumatriptan)

Migraine attack with or without aura.

Dosage regimen

Orally, the tablet should be swallowed whole with water. Begin treatment as soon as possible in case of a migraine attack. Recommended dose is 50 mg, if necessary - 100 mg.

If migraine symptoms do not disappear and do not decrease after the first dose, do not use this medicine repeatedly to stop the same attack.

To stop subsequent attacks (at symptom reduction or disappearance and then resumption), it is possible to take the second dose within next 24 hours, provided that the interval between doses is not less than 2 hours.

Maximum daily dose is 300 mg

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