Description
Pharmacological action
Pharmacotherapeutic group: anti-migraine.
ATC Code: [N02CC01]
Pharmacodynamics
Antimigraine agent. A specific and selective agonist of 5-HT1-serotonin receptors, localized mainly in the blood vessels of the brain, and does not affect other subtypes of 5-HT-serotonin receptors (5-HT2-7). It causes narrowing of the vessels of the carotid arterial bed, which supply extracranial and intracranial tissues with blood (dilation of the vessels of the meninges and / or their edema is the main mechanism for the development of migraine in humans), without significantly affecting the cerebral blood flow.
Suppresses activity of terminal receptors of afferent trigeminal fibers in the dura mater (as a result, the secretion of sensory neuropeptides is reduced). Eliminates nausea and photophobia associated with a migraine attack. In 50 ² 70% of cases, it quickly eliminates an attack when taken orally at a dose of 25-100 mg. Within 24 hours, in 1/3 of cases, relapse may develop, requiring repeated use.
Onset of action – 30 minutes after ingestion at a dose of 100 mg.
Pharmacokinetics
After oral administration, it is rapidly absorbed, after 45 minutes its plasma concentration reaches 70% of the maximum level. Bioavailability – 15% (due to presystemic metabolism and incomplete absorption). TCmax (after oral administration of 100 mg) is 2 ² 2.5 hours and amounts to 51 mg / ml.
Communication with plasma proteins – 14 ² 21%, total distribution volume – 170 l (2.4 l / kg).
Metabolized by oxidation with the participation of monoamine oxidase (MAO) (mainly isoenzyme A) with the formation of metabolites, the main of which are the indole acetic analog of sumatriptan, which does not have pharmacological activity with respect to 5-HT1 and 5-HT2 serotonin receptors, and its glucuronide.
T1 / 2 – 2 ² 2.5 hours. Plasma clearance – 1160 ml / min, renal clearance – 260 ml / min extrarenal clearance – 40% after ingestion. It is excreted by the kidneys, mainly in the form of metabolites (97% after ingestion) – a free acid or glucuronide conjugate.
Indications
Migraine (relieving seizures, with aura or bdriving her).
Contraindications
Hypersensitivity, hemiplegic, basilar or ophthalmoplegic forms of migraine, coronary heart disease (CHD), (including suspicion of it), angina pectoris (including Prinzmetal angina pectoris), including myocardial infarction history of arterial hypertension (uncontrolled), peripheral arterial occlusion, stroke or transient cerebrovascular accident (including history), liver and / or renal failure.
Precautions
Epilepsy (including any condition with a reduced epileptic threshold), arterial hypertension (controlled), pregnancy, lactation, childhood and adolescence (up to 18 years), advanced age (over 65 years), concomitant use of drugs (drugs) containing ergotamine and its derivatives, as well as MAO inhibitors and the period up to 14 days after their withdrawal.
Composition
Composition: 1 film-coated tablet contains:
active substance
sumatriptan succinate 70 mg and 140 mg. in terms of sumatriptan 50 mg and 100 mg
excipients:
hyprolose (hydroxy and propyl cellulose Klucel LF, calcium hydrogen phosphate dihydrate, mannitol (mannitol).
magnesium stearate. croscarmellose sodium (primellose),
microcrystalline cellulose
film composition:
Selecout AQ ² 02003 [hypromellose (hydroxypropyl methylcellulose), macrogol (6000 polyethylene glycol). titanium dioxide].
Dosage and Administration
Inside. Start treatment as soon as possible after a migraine attack (although the drug is equally effective at any stage of the attack). For the relief of acute migraine attacks for adults – 50 mg. if necessary, 100 mg (the tablet should be swallowed whole, washed down with water).
If the symptoms of migraine do not disappear and do not decrease after the first dose, then do not reappoint an ongoing attack to stop the attack. To stop subsequent attacks (with the reduction or disappearance of symptoms, and then resuming), you can take a second dose over the next 24 hours, provided that the interval between doses is at least 2 hours. During any 24 hours period, the maximum dose is 300 mg / day .
Side effects
From the cardiovascular system: decrease in blood pressure (BP), transient increase in blood pressure (observed shortly after administration), bradycardia. palpitations, tachycardia (including ventricular) in some cases – severe heart rhythm disturbances (up to ventricular fibrillation), transient changes in the ECG of ischemic type, myocardial infarction, in rare cases – Raynaud’s syndrome.
From the digestive system: nausea and vomiting in some cases, a slight increase in the activity of “liver” transaminases. discomfort in the abdomen, dysphagia, ischemic colitis.
On the part of the nervous system: dizziness, weakness (usually mild or moderate and transient) rarely – drowsiness, fatigue (more often when taken orally) in some cases – epileptic seizures (usually with a history of epilepsy).
On the part of the sensory organs: sometimes – diplopia, flickering flies before the eyes, nystagmus, scotoma, decreased visual acuity, very rarely – partial loss of vision (may be associated with the attack of migraine).
Allergic reactions: skin rash (including urticaria and erythematous rashes), itchy skin, anaphylactic reactions. Other: myalgia. “Flushing” of blood to the face.
Overdose
Symptoms: when ingested up to 400 mg, there are no other adverse reactions other than those listed above.
Treatment: observation of the patient for 10 hours, symptomatic therapy.
Storage conditions
List B. In a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
Expiration
3 years.
Deystvuyuschee substances
sumatriptan
dosage form
tablets
Kanonfarma, Russia
