Sumatriptan

Chemical name

3-[2-(Диметиламино)этил] -N-метилиндол-5-метансу льфонамид (and in the form of succinate)

Gross

C14-H21-N3-O2-S

Characteristics

White or no white powder, easily soluble in water and physiological solution.

Of drugs

The drugs-protivomigrenoznoe. Breakfast of migraine attack, but has a direct effect analgezirutm. Activates serotoninergicakie antinozitseptivee mechanisms barrel brain selectively initiates 5-HT_1D serotoninove receptors cerebrovascular (hard shell brain baziliarna artery), ingibiruet trigeminalna activation system, and reduces the accumulation of specific catalytic protein in the nuclei of troinicnogo nerve. It is a matter of narrowing expanded during the attack receptacle and thereby terminates Pristup.bystro and completely absorbed from the digestive tract, but the material is only 15%, due to presistemnogo metabolism. Biotransformiroetsa with MAO predominantly izofermenta A is the indolilazett and glukuronid. C_max when administered 100 mg is 51 ng / ml achieved within 2-2.5 hours (with migrenoznom amok slightly faster than mejpristupny period). The binding protein with the plasma low (14-21%). The average of 2.4 l / kg T_1/2-2.5 h, renal excretion of about 60%, the rest is with faeces. Report predominantly (97%) in the form of inactive metabolites. When s / to a dose of 6 mg C_max is about 75 ng / ml, the time for achieving 12 min. Bioavailability to 97%, the period of 15 minutes, T_1/2 the terminal phase-115 mines, the system Cl - 1.19 ml / min. The urine excreted 22% imposed dose, unedited, and 38% in indoliluksousna Kislota.bystro dosage attack in 50-70% of cases when administered in the dose of 25 to 100 mg. After 10-15 minutes after s / to the injections, after 15 minutes by intra or within 20 to 30 minutes after oral admission (maximum after one hour) terminated the worst attack, in a couple of hours to return to work. Alleviate associated with the attack migrenozna nausea and fotofobia. Most effective is the use of the altitude attack. About a third of cases in the next 24 hours can develop relapse, which makes re-use. The ingestion sometimes tranzitorno increases AD (as sistolicescoe or diastolicescoe).

Indications

Migraine (with fascination and without) : mild asthma and related symptoms; Horton syndrome.

Contraindications

Hypersensitivity, or baziliarnaya gemiplegical migraine, myocardial infarction, hypertonic kriz, arterial hypertension, stroke, ischemic heart disease (including bezbolevaya ischaemia), variantnaya vazospastical stenocardia, of the liver and kidney disease, pregnancy, breast-feeding, an elderly (over 60 years) and child.

Side-Effects

Pokalawania sense, pressure or gravity in the various parts of the body, hyperemia person, dizziness, weakness, drowsiness, and the AD pain for sternum stenocarditiceski nature, myocardial infarction, ventricular tachycardia, ventricular fibrillace, pain in the neck, mialgia, nausea, vomiting, discomfort in the abdomen, disfagia, burning in the nose or throat, active bleeding, eye irritation, impaired vision, pain at the injection.

Precautions

Before and during the course of treatment necessary to the diet to eat regularly, delete products containing tiramin (chocolate, cocoa, nuts, citrus fruits, beans, tomatoes, celery, cheese), as well as alcoholic beverages (including dry, especially red wine, champagne, beer), maintain a healthy lifestyle, sports (swimming, skiing, walking), to have a passion, a hobby, which creates a positive emotional state, and thereby prevents the emergence of migrenozhnykh attacks. Because of the possible acute coronary arteries, especially in patients with ischemic heart disease and elderly patients, the first 2-3 admission must be under medical supervision. There should be combined with drugs ergotamine. People with a fixed sulfanilamidna eritema in history increases the risk of allergic reactions. Be wary designate drivers and employees potentially hazardous activities that require greater attention and speed of reaction.

Dosing and Administration

Inside, c / a, route. P / for the special injectors (possibly independent of patients) in the dose of 6 mg, if necessary through 6.3.13 again (maximum daily dose of 12 mg); Inwards on 50-100 mg (no more than three tables. A day at intervals of not less than 1 hour); Horton syndrome, p / of the dose of 6 mg every amok. Intranasal 1 dose (10 or 20 mg), the re-introduction may at intervals of not less than 2 hours

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