Expiration date: 12/2025
Composition
sumatriptan 50 or 100 mg
excipients: hyprolose (GI the gorse and propyl cellulose LF Klucel, calcium hydrogen phosphate dihydrate, mannitol (mannitol). magnesium stearate. croscarmellose sodium (Primerose), cellulose microcrystalline,
Pharmacological action
Anti-migraine agent. Specific and selective agonist of 5-HT1-serotonin receptors localized mainly in blood vessels of the brain, and has no effect on other subtypes of 5-HT serotonin receptors (5-HT2–7). Causes vasoconstriction of the carotid arterial bed, which supply blood to extracranial and intracranial tissues (expansion of blood vessels of the meninges and/or swelling is the main mechanism of development of migraine in humans) without significant effect on cerebral blood flow.
Inhibits the activity of receptor endings of the afferent fibers of the trigeminal nerve in the Dura mater (resulting in a decrease in the allocation of sensory cortex). Addresses associated with migraine attack with nausea and photophobia. In 50-70% cases quickly resolves the attack when administered in a dose of 25-100 mg. for 24 hours in 1/3 of cases may develop a recurrence requiring re-application.
Onset of action is 30 minutes after ingestion in a dose of 100 mg.
Pharmacokinetics
After intake of rapidly absorbed, 45 min later its concentration in plasma reaches 70% of maximum level. Bioavailability 15% (due to presystemic metabolism and incomplete absorption). TCmax (after intake of 100 mg) — 2-2.5 h and is 51 mg/ml.
Connection with plasma proteins — 14-21%, and the total volume of distribution is 170 litres (2.4 l/kg).
Metabolized by oxidation with the participation of monoamine oxidase (MAO) (primarily the isoenzyme A) with the formation of metabolites, the main escoteric are indelicacy analogue of sumatriptan, which do not possess pharmacological activity against 5-HT1 and 5-HT2 serotonin receptors, and its glucuronide.
T1/2 — 2-2.5 h. Plasma clearance is 1160 ml/min, kidney klirens — 260 ml/min, extrarenal clearance — 40% after ingestion. Excreted by the kidneys, mainly as metabolites (97% after ingestion) is a free acid or as glucuronide conjugate.
Side effects
From the cardiovascular system: lower blood pressure (BP), a transient increase in blood pressure (observed soon after admission), and bradycardia. palpitations, tachycardia (including ventricular), in some cases, severe cardiac arrhythmias (up to ventricular fibrillation), transient ECG changes ischemic-type, myocardial infarction, and in rare cases — Raynaud's syndrome.
From the digestive system: nausea and vomiting, in some cases, a slight increase in activity "liver" transaminases. a feeling of abdominal discomfort, dysphagia, ischemic colitis.
From nervous system: dizziness, weakness (usually weakly or moderately expressed and are transient), rarely — drowsiness, feeling tired (usually by ingestion), in some cases, epileptic seizures (usually when you have a history of epilepsy).
From the sensory organs: sometimes — double vision, flashing flies before the eyes, nystagmus, scotoma, reduced visual acuity, rarely — blurred vision (can be connected to a migraine attack).
Allergic reactions: skin rash (including urticaria and erythematous rash), itching, anaphylactic reactions. Other: myalgia. "tides" of blood to the face.
Special conditions
Not intended to prevent migraines (administration during a migraine aura prior to the occurrence. symptoms may not prevent the development of headaches).
Patients risk group for cardio vascular system therapy do not begin without preliminary survey (women in post-menopausal stages, men over the age of 40 years. persons with risk factors for CHD).
In the appointment during lactation is not recommended to breast feed for 24 h after administration of sumatriptan.
In patients with hypersensitivity to sulfonamides with the introduction of sumatriptan increased risk of allergic reactions (cutaneous manifestations to anaphylactic shock).
In the absence of effect of the first dose administration should clarify the diagnosis.
Experience with the use of sumatriptan in patients over 65 years is limited (significant difference in pharmacokinetics compared to younger patients is not observed).
Before prescribing sumatriptan, patients with newly diagnosed or occurring atypical migraine to exclude other potentially dangerous neurological disease.
It must be borne in mind that patients suffering from migraine there is a risk of stroke and transient disorders of cerebral circulation.
During the period of treatment must be careful when driving and occupation of other potentially hazardous activities, require high concentration and psychomotor speed reactions.
Testimony
Migraine (mild asthma, with aura or without it).
Contraindications
Hypersensitivity, hemiplegic, basilar or oftalmologicheskiy forms of migraine, ischemic heart disease (IHD) (including suspected it), angina (including Prinzmetal's angina), myocardial infarction (including history), hypertension (uncontrolled), occlusal peripheral artery disease, stroke or transient disorders of cerebral circulation (including in history), liver and/or kidney failure.
Drug interactions
Simultaneous administration with ergotamine and ergotaminsoderjasimi LS possible long-term spasm of the vessels (the interval between their admission must be at least 24 hours).
Perhaps the interaction between sumatriptanom and MAO inhibitors (to decrease the intensity of metabolism of sumatriptan, increasing its concentration).
While the use of sumatriptan and drugs from the group of selective inhibitors of serotonin reuptake may develop weakness, hyperreflexia and poor coordination of movements
