Sumatriptan - instructions for use, dose, side effects, contraindications

Excipients: giprolose (hydroxypropyl cellulose Klucel LF, calcium hydrophosphate dihydrate, mannitol (mannitol), magnesium stearate, croscarmellose sodium (impellose), microcrystalline cellulose;

composition of film shell: Selobout AQ-02003 [hypromellose (hydroxypropylmethylcellulose), macrogol (polyethylene glycol 6000), titanium dioxide].

Description:

The tablets covered with a film membrane of white or almost white color, round, biconcave form.

Pharmacotherapeutic group:Anti-migraine means.

ATX: & nbsp

N.02.C Anti-migraine drugs

Pharmacodynamics:

Anti-migraine means. Specific and selective agonist of 5-HT1-serotonin receptors, localized predominantly in the blood vessels of the brain, and does not affect other subtypes of 5-HT-serotonin receptors (5-HT2-7). Causes narrowing of the vessels of the carotid arterial bed, which supply extracranial and intracranial tissues (the expansion of the vessels of the meninges and / or their edema is the main mechanism of migraine development in humans) without significantly affecting cerebral blood flow.

Suppresses the activity of the receptors of the endings of the afferent fibers of the trigeminal nerve in the dura mater (as a result, the secretion of sensory neuropeptides decreases).Eliminates the associated nausea and photophobia associated with migraine attacks. In 50-70% of cases, it quickly eliminates an attack with oral administration in a dose of 25-100 mg. Within 24 hours, a relapse may occur in 1/3 of the cases requiring re-application.

The onset of action is 30 minutes after oral administration at a dose of 100 mg.

Pharmacokinetics:

After oral intake quickly absorbed, after 45 minutes its concentration in the plasma reaches 70% of the maximum level. Bioavailability - 15% (due to presystemic metabolism and incomplete absorption). TSshah (after ingestion 100 mg) - 2-2.5 hours and is 51 ng / ml.

The connection with plasma proteins is 14-21%, the total volume of distribution is -170 l (2.4 l / kg).

Metabolized by oxidation with the participation of monoamine oxidase (MAO) (preferably isoenzyme A) to form metabolites, the main ones being the indoleacetic analogue of sumatriptan, not having pharmacological activity against 5-HT1 and 5-HT2-serotonin receptors, and its glucuronide.

T1 / 2 - 2-2.5 hours. Plasma clearance - 1160 ml / min, renal clearance - 260 ml / min; non-adrenal clearance - 40% after oral administration. It is excreted by the kidneys, mainly in the form of metabolites (97% after ingestion) - free acid or glucuronide conjugate.

Indications:Migraine (relief of seizures, with or without an aura).

Contraindications:Hypersensitivity, hemiplegic, basilar or ophthalmoplegic forms of migraine, ischemic heart disease (IHD), (including suspected of it), angina (including angina of Prinzmetal), myocardial infarction (including in the anamnesis) , arterial hypertension (uncontrolled), occlusive diseases of peripheral arteries, stroke or transient impairment of cerebral circulation (including in anamnesis), hepatic and / or renal insufficiency.

Carefully:Epilepsy (including any condition with a reduced epileptic threshold), arterial hypertension (controlled), pregnancy, lactation, children and adolescence (under 18), elderly (more than 65 years); simultaneous administration of medications (LS) containing ergotamine and its derivatives, as well as MAO inhibitors and up to 14 days after their cancellation.

Dosing and Administration:

Inside. Begin treatment as early as possible after the onset of a migraine attack (although the drug is equally effective at any stage of the attack). For relief of acute migraine attacks adults - 50 mg, if necessary - 100 mg (the tablet should be swallowed whole, washed down with water).

If migraine symptoms do not disappear and do not decrease after the first dose, then repeatedly to stop the ongoing attack is not prescribed. To stop subsequent attacks (with a decrease or disappearance of symptoms and then resume), you can take a second dose within the next 24 hours, provided that the interval between admission is at least 2 hours. During any 24 hours of the period, the maximum dose is 300 mg / day .

Side effects:

From the side of the cardiovascular system: lowering blood pressure (BP), transient increase in blood pressure (observed soon after administration), bradycardia, palpitation, tachycardia (including ventricular); in some cases - severe disturbances of the heart rhythm (up to ventricular fibrillation), transient ECG changes 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, a feeling of discomfort in the abdomen, dysphagia, ischemic colitis.

From the nervous system: dizziness, weakness (usually mild or moderately expressed and transient); rarely - drowsiness,a feeling of fatigue (more often with ingestion); in some cases - epileptic seizures (usually with a history of epilepsy).

From the sense organs: sometimes - diplopia, flickering flies before the eyes, nystagmus, scotoma, visual acuity reduction, very rarely - partial loss of vision (may be associated with the migraine attack itself).

Allergic reactions: skin rash (including hives and erythematous rashes), skin itching, anaphylactic reactions. Other: Myalgia, "tides" of blood to the face.

Overdose:

Symptoms: when ingesting up to 400 mg, no other adverse reactions are noted other than those listed above.

Treatment: observation of the patient within 10 hours, symptomatic therapy.

Interaction:

With simultaneous administration with ergotamine and ergotamine-containing JIC, a prolonged vasospasm can occur (the interval between their intake should be at least 24 h).

Possible interaction between sumatriptan and MAO inhibitors (decrease in the intensity of metabolism of sumatriptan, increasing its concentration).

With the simultaneous use of sumatriptan and LS from the group of selective serotonin reuptake inhibitors, weakness, hyperreflexia and coordination disorders may develop.

Special instructions:

It is not intended for the prevention of migraine (introduction during the migraine aura before the onset of other symptoms may not prevent the development of a headache).

Patients at risk for the cardiovascular system do not begin therapy without a preliminary examination (postmenopausal women, men over the age of 40, persons with IHD risk factors).

At appointment in a lactemia it is not recommended to breastfeed within 24 hours after taking sumatriptan.

In patients with hypersensitivity to sulfonamides with the introduction of sumatriptan, there is an increased risk of allergic reactions (from skin manifestations to anaphylactic shock).

If there is no effect on the administration of the first dose, the diagnosis should be clarified.

The experience with sumatriptan in patients older than 65 years is limited (there is no significant difference in pharmacokinetics compared with younger patients).

Before prescribing sumatriptan, patients with newly diagnosed or atypically migraine should exclude other potentially dangerous neurological diseases.

It should be borne in mind that in patients suffering from migraine, there is a risk of developing a stroke or transient disorders of the cerebral circulation.

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 50 mg and 100 mg.

Packaging:

By 2, 4, 6, 10 tablets in a contour mesh box made of polyvinyl chloride film and aluminum foil printed lacquered.

On 1 contour acheikova packing together with the instruction on application place in a pack from a cardboard.

Storage conditions:List B. In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003583/09

Date of registration:14.05.2009

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Information update date: & nbsp06.09.2015

Illustrated instructions

Instructions

Sumatriptan (Sumatriptan)