Суматриптан

Description

Sumatriptan is a selective agonist of serotonin receptor subtypes 5-HT1B and 5-HT1D, the first substance in the triptan class. According to the anatomical-therapeutic-chemical classification, it is assigned to code N02CC01, a group of selective agonists of serotonin 5-HT1 receptors, section N - nervous system. Chemically, it is an indole derivative with a methanesulfonamide group at position 5 and a dimethylaminoethyl substituent at position 3.

Identification

• CAS No: 103628-46-2
• Chemical formula: C14H21N3O2S
• English name: Sumatriptan
• Systematic name: 3-[2-(dimethylamino)ethyl]-N-methyl-1H-indole-5-methanesulfonamide
• Molecular weight: 295.4
• Exact weight: 295.40
• UNII: 8R78F6L9VO
• DSSTox ID: DTXSID4023628
• NCI Thesaurus Code: C1240
• ATC code: N02CC01, section N - nervous system
• HS code: 2935904000
• Laboratory developer codes: GR 43175, GR 43175X

Mechanism of action

The substance binds to 5-HT1B receptors on the smooth muscle of cranial vessels and to 5-HT1D receptors on the presynaptic terminals of the trigeminal nerve. There are two results: narrowing of the dilated vessels of the dura mater and inhibition of the release of vasoactive neuropeptides that support neurogenic inflammation during a migraine attack. Affinity for 5-HT2 and 5-HT3 receptors, as well as adrenergic, dopamine and muscarinic receptors is low, so the action profile is narrow.

Purpose

Pharmaceutical substance for the production of drugs that relieve migraine attacks with and without aura, as well as cluster headache attacks. Triptans act on an attack that has already begun and are not used for prevention.

Dosage forms and trade names

The substance is processed into salt (usually succinate) and introduced into forms with different rates of onset of effect. The list of card synonyms contains trade designations, each of which corresponds to its own form of delivery:

• Zelrix and Zecuity - transdermal system
• Onzetra Xsail - intranasal powder
• GR 43175 - original designation of the developer

Synonyms

• 1H-Indole-5-methanesulfonamide, 3-[2-(dimethylamino)ethyl]-N-methyl-
• 3-[2-(Dimethylamino)ethyl]-N-methyl-1H-indole-5-methanesulfonamide
• 1-[3-[2-(Dimethylamino)ethyl]-1H-indol-5-yl]-N-methylmethanesulfonamide

Storage and handling

Storage conditions and transport codes are not given in the original product card; they are set by the specifications of a particular manufacturer of the substance. Handling - according to the rules for working with pharmaceutical substances: closed containers, protection from moisture, dust control during hanging, incoming control according to the quality certificate and certificate of analysis.