SUMATRIPTAN (Sumatriptan).

     3-[2 - (Dimetilamino) ethyl] -N- metindol-5- metansulfonamida succinate.

     Synonyms : Imigran, Imitreks, Imigran, Imitrex.

     White or almost white powder. The easily soluble in water.

     TiHKAL synthetic derivative, is structurally similar to serotonin, a (1989) to find specific antimigrenevogo funds. The reason for its creation as a modern vision of the role of serotonin (5-mainly NT1) receptors in the regulation of vascular tone brain. It has been shown that a selective agonist sumatriptan 5-NT1 D receptor stimulation which weakens the brain pulsation vessels and related headache. The drug also reduces the release of brain and other mediators of inflammation.

     At adrenergicheskie, dofaminergicheskie, muskarinovye and benzodiazapine sumatriptan receptors expressed no influence. Direct action does not have blood.

     When ingestion rapidly and completely absorbed in the digestive tract, bioavailability of approximately 12% as a result of "first pass effect" through the liver (with subcutaneous introduction of 100%), C max, 2-2? h, T? - 2.5 h; out with urine and faeces.

     Applied to cupping the migraines. Preparation is usually quickly removes or reduces headaches (with or without aura). Decreases also nausea, vomiting, photophobia, and other phenomena associated with migraine attacks. You can assign oseltamivir with frequent migraine attacks, but for long-term preventive use is not recommended. Usually effective in patients not responding to nenarkoticheskie analgesics and NPVS.

     Assign inside, and subcutaneously route.

     Inside apply beginning with a single dose of 0,05-0,1 g (50 and 100 mg). With insufficient effects used again in the same dose in 1 hour (no more than 0.3 grams per day).

     Under the skin (hip or forearm) are (using special syringes) in the dose of 0,006 grams (6 mg); Through one hour and you can repeat the same dose. When bad Portability impose a lesser dose. The total dose of 0,012 grams should not be more than 24-48 hours

     Intranasal impose on one dose (0,01-0,02 g), with an interval of 2 hours

     Usually migraine attack goes through 10-15 minutes after subcutaneous and intranasal and over 20-60 min after oral delivery.

     Using the drug could experience Blush person, headache, pain in the heart and neck, zheludochkovye adults, difficulty swallowing, lack of a sense of air, muscle pain; Not eliminated allergic reactions and other side effects that are themselves.

     It should not be used in conjunction with sumatriptan MAO inhibitors (antidepressants, furazolidonom, prokarbazinom, selegilinom) - inhibitor antidepressants neyronalnogo Serotonin (see Fluoxetine).

    The drug is not suitable for measuring heart disease after myocardial infarction and deferred disturbance of cerebral circulation, in violation of the liver and kidney, epilepsy, pregnancy and breastfeeding, in old and young age.

     Before and during treatment must comply with the diet removed from the food products containing tiramin (chocolate, cocoa, nuts, citrus fruit, beans, tomatoes, cheese, etc.).

     Be wary designate drivers and others whose work requires more attention and reaction speed.

     Method of production : tablets of 0.05 and 0.01 g (50 and 100 mg N) (2); 1.2% injection of 0.5 ml of syringes (N 2); Aerosol intranasal ( 10, and 20 mg / dose).

     Storage : List B.

     The complexity of cerebrovascular and biochemical mechanisms of pathogenesis of migraine is difficult to expect that drugs are selectively acting only serotoninergicheskie processes can be uniformly treatment of the disease.

     In different stages of migraine are complex changes mediator processes : the content of cerebral vascular catecholamines and serotonin, MAO activity, etc.; Been shrinking, and then increased cerebral vascular; Swelling is accompanied by the release of vascular wall vazodilatatornyh active peptide, aggregation of platelets increased. Symptoms vary in appearance and clinical manifestations of disease.

     Currently, cupping the migraine usually apply NPVS - atsetilsalitsilovuyu acid (aspirin) and containing a combination of drugs, especially digidrirovannye derived alkaloids LPV (see Digidroergotamin). Long used in migraine derived alkaloids LPV have complex regulatory (mainly vazokonstriktornoe) effect on the brain vessels and influence on serotoninergicheskie and adrenergicheskie processes.

     Sumatriptan and its analogs significantly enhance pharmacotherapy (mild stroke), migraines, it is necessary, however, the further accumulation of data on the effectiveness and mechanisms of this new group LS.

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