Sumatriptan Canon pills 50mg, 2pcs

Composition

Film-coated tablets,50 mg and 100 mg. 2,4,6,10 tablets in a contour cell package made of polyvinyl chloride film and aluminum foil printed varnished.

1 contour cell package together with the instructions for use is placed in a pack of cardboard.

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 (gi drocke and propyl cellulose Klucel LF, calcium hydrophosphate dihydrate, mannitol (mannitol).

magnesium stearate. croscarmellose sodium (primellose),

microcrystalline cellulose;

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

Pharmacological action

Anti-migraine medication. It is a specific and selective agonist of 5-HT-1 serotonin receptors located mainly in the blood vessels of the brain, and does not act on other subtypes of 5-HT-serotonin receptors (5-HT 2-7).

Causes vasoconstriction of the carotid arterial bed, which supplies blood to extracranial and intracranial tissues (vasodilation of the meninges and / or their edema is the main mechanism of migraine development in humans), without significantly affecting the cerebral blood flow.

Inhibits the activity of receptors of the endings of the afferent fibers of the trigeminal nerve in the dura mater (as a result, the release of sensory neuropeptides decreases). Eliminates nausea and photophobia associated with a migraine attack. In 50-70% of cases, it quickly eliminates an attack when taken orally at a dose of 25-100 mg. Within 24 hours,1/3 of cases may develop a relapse that requires repeated use.

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

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

Plasma protein binding was 14-21%, and the total volume of distribution was 170 l (2.4 l / kg).

It is metabolized by oxidation with the participation of monoamine oxidase (MAO) (mainly isoenzyme A) with the formation of metabolites, the main of which are the indoleacetic analog of sumatriptan, which does not have pharmacological activity against 5-HT1 – and 5-HT2-serotonin receptors, and its glucuronide.

T 1/2-2-2.5 h. Plasma clearance-1160 ml / min, renal clearance-260 ml / min; extrarenal clearance-40% after oral use. Excreted by the kidneys, mainly in the form of metabolites (97% after oral use) — free acid or glucuronide conjugate.

Indications

Migraine (relieving seizures, with or without aura).

Contraindications

Hypersensitivity, hemiplegic, basilar or ophthalmoplegic forms of migraines, coronary heart disease (CHD), (including suspected), angina (including Prinzmetal angina), myocardial infarction (including in the anamnesis), arterial hypertension (uncontrolled), occlusive diseases of the peripheral arteries, stroke or transient cerebrovascular accident (including in the case of medical history), hepatic and/or renal failure.

With caution

Epilepsy (including any conditions with a reduced epileptic threshold), arterial hypertension (controlled), pregnancy, lactation, childhood and adolescence (up to 18 years), the elderly (over 65 years); simultaneous use of medicines containing ergotamine and its derivatives, as well as MAO inhibitors and up to 14 days after their withdrawal.

Side effects

From the cardiovascular system:  decreased blood pressure( BP), transient increase in blood pressure (observed shortly after use), bradycardia. palpitations, tachycardia (including ventricular); in some cases — severe cardiac arrhythmias (up to ventricular fibrillation), transient ECG changes of the ischemic type, myocardial infarction, in isolated cases — Raynaud’s syndrome.

From the digestive system:  nausea and vomiting; in some cases-a slight increase in the activity of” hepatic ” transaminases. abdominal discomfort, dysphagia, ischemic colitis.

Nervous system disorders:  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).

From the side of the senses:  sometimes-diplopia, flickering of flies in front of the eyes, nystagmus, scotoma, decreased visual acuity, very rarely-partial loss of vision (may be associated with the migraine attack itself).

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

Interaction

When administered concomitantly with ergotamine and ergotamine-containing drugs, prolonged vascular spasm is possible (the interval between their use should be at least 24 hours).

Interaction between sumatriptan and MAO inhibitors is possible (decrease in the intensity of sumatriptan metabolism, increase in its concentration).

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

How to take, course of use and dosage

Inside. Start treatment as early as possible after a migraine attack occurs (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 again to stop the ongoing attack is not prescribed. To stop subsequent attacks (if symptoms decrease or disappear, and then resume), you can take a second dose within the next 24 hours, provided that the interval between use is at least 2 hours. During any 24-hour period, the maximum dose is 300 mg / day.

Overdose

Symptoms:  when taken orally up to 400 mg, no other side effects are observed, except for those listed above.

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

Special instructions

It is not intended for the prevention of migraines (use during a migraine aura before other symptoms occur may not prevent the development of headaches).

Patients at risk from the cardiovascular system should not start therapy without a preliminary examination (women in the postmenopausal period, men over the age of 40 years. individuals with CHD risk factors).  

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

Patients with hypersensitivity to sulfonamides with the introduction of 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.

The experience of using sumatriptan in patients over 65 years of age is limited (there is no significant difference in pharmacokinetics compared to younger patients).

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

It should be borne in mind that patients suffering from migraines are at risk of developing a stroke or transient disorders of the cerebral circulation.

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

Form of production

film-coated tablets of white or almost white color, round, biconvex shape.

Storage conditions

Keep out of reach of children. In a dry place protected from light at a temperature not exceeding 25°C.

Shelf

life is 2 years.

Active ingredient

Sumatriptan

Conditions of release from pharmacies

By prescription

Dosage form

Tablets