Sumatriptan Canon, 50 mg 2 pcs

Antimigraine medication. Specific and selective agonist of 5-NT1-serotonin receptors, localized mainly in blood vessels of the brain, and does not act on other subtypes of 5-NT-serotonin receptors (5-NT2-7).

It causes narrowing of the carotid arterial bed vessels, which supply blood to the extracranial and intracranial tissues (dilation of the cerebral membrane vessels and/or their edema is the main mechanism of migraine development in humans), while not having a significant effect on cerebral blood flow.

Suppresses the activity of receptors of trigeminal nerve afferent fibers endings in the dura mater (as a result the release of sensory neuropeptides is reduced). It eliminates nausea and photophobia associated with migraine attack. In 50-70% of cases it quickly eliminates the attack when taken orally in a dose of 25-100 mg. Within 24 h, in 1/3 of cases a relapse may occur, requiring reapplication.

The onset of action is 30 minutes after an oral dose of 100 mg.

Pharmacokinetics

After oral administration it is rapidly absorbed, after 45 min its concentration in plasma reaches 70% of the maximum level. Bioavailability is 15% (due to presystemic metabolism and incomplete absorption). TCmax (after oral administration of 100 mg) is 2-2.5 h and is 51 mg/ml.

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

It is metabolized by oxidation with the help of monoamine oxidase (MAO) (mainly isoenzyme A) with formation of metabolites, basic of which are indole acetic analog of sumatriptan without pharmacological activity against 5-HT1- and 5-HT2-serotonin receptors and its glucuronide.

The T1/2 is 2-2.5 h. Plasma clearance is 1160 ml/min, renal clearance is 260 ml/min; extra-renal clearance is 40% after oral administration. Excreted by the kidneys, mainly as metabolites (97% after oral administration) – free acid or glucuronide conjugate.

Indications

Migraine (control of attacks, with or without aura).

Active ingredient

Composition

Film-coated tablets, 50 mg and 100 mg. 2, 4, 6, 10 tablets in a polyvinyl chloride film and aluminum foil lacquered.

1 contour cell pack, along with instructions for use, is placed in a carton pack.

1 film-coated tablet contains:

active ingredient

sumatriptan succinate 70 mg and 140 mg. In terms of sumatriptan 50 mg and 100 mg;

excipients:

Hyprolose (hy drocke and propyl cellulose Clucel LF, calcium hydrophosphate dihydrate, mannitol (mannitol).

Magnesium stearate. croscarmellose sodium (primellose),

particle cellulose microcrystalline;

composition of the film coating: Selecoat AQ-02003 [hypromellose (hydroxypropyl methylcellulose), macrogol (polyethylene glycol 6000). titanium dioxide].

How to take, the dosage

Ingestion. Begin treatment as soon as possible after a migraine attack (although the drug is equally effective at any stage of the attack). For relief of acute migraine attacks in adults – 50 mg. if necessary – 100 mg (the tablet should be swallowed whole with water).

If migraine symptoms do not disappear and do not decrease after the first dose, do not use repeatedly to stop an ongoing attack. For control of subsequent attacks (when symptoms decrease or disappear and then resume) a second dose may be administered within the next 24 hours, provided that the interval between doses is at least 2 hours. During any 24 h period, the maximum dose is 300 mg/day.

Interaction

In concomitant administration with ergotamine and ergotamine-containing drugs prolonged vasospasm is possible (interval between their administration should be at least 24 hours).

Possible interaction between sumatriptan and MAO inhibitors (decreased intensity of sumatriptan metabolism, increased concentration).

In concomitant use of sumatriptan and drugs from the group of selective serotonin reuptake inhibitors, weakness, hyperreflexia and impaired coordination of movements may occur.

Special Instructions

It is not intended for migraine prophylaxis (administration during migraine aura before occurrence of other symptoms may not prevent development of headache).

To patients of cardiovascular risk group therapy should not be started without prior examination (women in the postmenopausal period, men over 40 years old. Individuals with risk factors for CHD).

When prescribing during lactation, it is not recommended to breastfeed the child for 24 hours after taking sumatriptan.

Patients with hypersensitivity to sulfonamides when administering sumatriptan have an increased risk of allergic reactions (from skin manifestations to anaphylactic shock).

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

Limited experience with sumatriptan in patients over 65 years of age (no significant difference in pharmacokinetics compared to younger patients).

Before prescribing sumatriptan to patients with newly diagnosed or atypical migraine, other potentially dangerous neurological diseases should be excluded.

It should be borne in mind that patients with migraine are at risk of developing stroke or transient cerebral circulatory disturbances.

When treating, caution should be exercised when driving motor vehicles and engaging in other potentially hazardous activities that require increased concentration and quick psychomotor reactions.

Contraindications

Hypersensitivity, hemiplegic, basilar or ophthalmoplegic forms of migraine, coronary heart disease (CHD), (including suspected), angina pectoris (including Prinzmetal angina), myocardial infarction (including history), arterial hypertension (uncontrolled), peripheral arterial occlusive disease, stroke or transient cerebral circulation disorder (including history), hepatic and/or renal insufficiency.

With caution

Epilepsy (including. any condition with reduced epileptic threshold), arterial hypertension (controlled), pregnancy, lactation, childhood and adolescence (under 18 years), old age (over 65 years); simultaneous use of drugs (drugs) containing ergotamine and its derivatives and MAO inhibitors and the period up to 14 days after their withdrawal.

Side effects

Cardiovascular system: decrease of arterial pressure (BP), transient increase of BP (observed soon after administration), bradycardia, palpitation, tachycardia (including ventricular); in some cases – severe cardiac rhythm disturbances (up to ventricular fibrillation), transient ischemic ECG changes, myocardial infarction, in single cases – Raynaud’s syndrome.

Digestive system disorders: nausea and vomiting; in some cases – minor increase in “hepatic” transaminase activity, feeling of discomfort in the stomach, dysphagia, ischemic colitis.

Nervous system disorders: dizziness, weakness (usually mild to moderate and transient); rarely – drowsiness, fatigue (more often when taken orally); epileptic seizures in individual cases (usually with a history of epilepsy).

Senses: sometimes – diplopia, flickering of flickers before eyes, nystagmus, scotoma, decreased visual acuity, very rare – partial loss of vision (may be associated with the attack of migraine itself).

Allergic reactions: skin rash (including urticaria and erythematous rash), skin itching, anaphylactic reactions.Other: myalgia. “flushes” of blood to the face.

Overdose

Symptoms: no adverse reactions other than those listed above are observed when ingested up to 400 mg.

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

Similarities