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

Composition
Sumatriptan succinate -	70 mg	140 mg
in terms of sumatriptan -	50 mg	100 mg
Auxiliary substances:
lactose (milk sugar), -	192 mg	215.5 mg
calcium hydrophosphate - 30 mg 34 mg (calcium phosphate disubstituted) magnesium stearate, 3 mg 4 mg Povidone 5 mg 6.5 mg Average tablet weight without - 300 mg 400 mg shells Auxiliary substances for the shell: hypromellose 7 mg 10.5 mg (hydroxypropyl- methyl cellulose), Copovidone (copolyvidone), 1 mg of 1.5 mg polyethylene glycol 6000 - 1 mg 1.5 mg (macrogol) talc, - 0.5 mg 0.75 mg
titanium dioxide, - dye crimson - [Ponso 4R] The average weight of a tablet with a shell	0.45 mg	0.75 mg
	0.05 mg 0.0mg 310 mg 415 mg

Description:The tablets covered with a film covering of pink color, round, biconcave form (for a dosage of 50 mg), white or white with kremovatym a shade of color, biconcave form, oblong with the rounded ends, with a risk (for a dosage of 100 mg). On the fracture, the inner layer is white.

Pharmacotherapeutic group:Anti-migraine means.

ATX: & nbsp

N.02.C Anti-migraine drugs

Pharmacodynamics:

Sumatriptan is a specific selective agonist of vascular 5- hydroxytryptamine-1 receptors (5HT_ID), does not affect other subtypes of 5HT-serotonin receptors (5HT₂ - 5HT₇). 5HT Receptors_ID are located, mainly, in the blood vessels of the brain, and their stimulation leads to narrowing of these vessels. Reduces the sensitivity of the trigeminal nerve.Both these effects can underlie the anti-migraine effect of sumatriptan. The clinical effect is usually observed after 30 minutes after oral administration of the drug.

Pharmacokinetics:

After oral administration sumatriptan quickly absorbed, 70% of the maximum plasma concentration is achieved after 45 minutes. After taking 100 mg, the maximum concentration in the blood plasma is on the average 54 mg / ml. Bioavailability is 14% due to intensive pre-systemic metabolism and incomplete absorption. The connection with plasma proteins is low (14-21%). Sumatriptan is metabolized by the action of monoamine oxidase A. The main metabolite, indoleacetic analogue of sumatriptan, is excreted predominantly in urine, in the form of free acid and glucuronide conjugate. This metabolite has no activity in relation to 5HT₁ - and 5HT₂ -serotonin receptors.

Indications:Coping migraine attacks with or without an aura.

Contraindications:

- Hypersensitivity to any component of the drug.

- Hemiplegic, basilar and ophthalmoplegic forms of migraine.

- Ischemic heart disease (IHD) (including myocardial infarction, postinfarction cardiosclerosis, Prinzmetal angina), as well as the presence of symptoms suggesting the presence of IHD.

- Occlusal diseases of peripheral vessels.

- Stroke or transient ischemic attack (including in anamnesis).

- Use of monoamine oxidase inhibitors (MAO) or earlier than 2 weeks after the withdrawal of these drugs.

- Uncontrolled hypertension.

- Admission simultaneously with ergotamine or its derivatives (including metisergid).

- Severe dysfunction of the liver and / or kidney.

- Age 18 years and over 65 years of age (safety and efficacy of sumatriptan not established).

- Pregnancy and lactation.

Carefully:

- controlled arterial hypertension;

- diseases in which the absorption, metabolism or excretion of this drug can change (eg, impaired renal or hepatic function);

- epilepsy (including any conditions with a decrease in the threshold of convulsive readiness);

- in patients with hypersensitivity to sulfonamides (administration of sumatriptan can cause allergic reactions, the severity of which varies from skin manifestations to anaphylaxis.) Data on cross-sensitivity are limited, but caution should be exercised when assigning sumatriptan to such patients).

Dosing and Administration:

Inside, swallowing the tablet whole and squeezed water. If not prescribed otherwise: the recommended dose is one 50-mg tablet. Some patients may require a higher dose of 100 mg. If migraine symptoms do not disappear and do not decrease after taking the first dose, then for cupping the same An attack should not be repeated. However, the drug can be used for cupping subsequent migraine attacks.

If the patient senses a decrease or disappearance of symptoms after the first dose, and then the symptoms resume, a second dose can be taken within the next 24 hours, provided that the interval between admissionis at least 2 hours. The maximum dose of sumatriptan should not exceed 300 mg during the 24-hour period.

Side effects:

Are common

Pain, a feeling of squeezing or heaviness, a feeling of heat or tingling in various parts of the body.

Tides, dizziness, a feeling of weakness, a feeling of fatigue, drowsiness is usually expressed weakly or moderately and is of a transient nature.

From the side of the cardiovascular system

Reduced blood pressure, bradycardia, tachycardia, a transient increase in blood pressure (observed soon after taking sumatriptan).Rarely - violations of the heart rate, transient ECG changes in the ischemic type, myocardial infarction, spasm of the coronary arteries. Sometimes Raynaud's syndrome develops.

From the gastrointestinal tract

Nausea, vomiting, ischemic colitis (but the relationship of these side effects with sumatriptan is not established); dysphagia, a feeling of discomfort in the abdomen.

From the side of the central nervous system and sensory organs

Dizziness, rarely convulsive seizures (in a number of cases they were observed in patients with a history of seizures or in conditions predisposing to the occurrence of seizures, in some patients predisposing factors were not found). Sometimes after taking sumatriptan, there is diplopia, flashing before the eyes, nystagmus, scotoma, visual acuity reduction. Very rarely develops a partial transient loss of vision. However, it should be borne in mind that visual impairment can be associated with the very seizure of a migraine.

Hypersensitivity reactions

Varies from skin manifestations (rash, hives, itching, erythema) to rare cases of anaphylaxis.

From the laboratory indicators

Minor changes in the activity of "liver" transaminases.

Overdose:

Taking sumatriptan inside at a dose of more than 400 mg did not cause any side effects other than those listed above.

In case of an overdose, patients should be monitored for at least 10 hours and, if necessary, symptomatic therapy should be performed. There is no data on the effect of hemodialysis or peritoneal dialysis on the concentration of sumatriptan in plasma.

Interaction:

No interaction of sumatriptan with propranolol, flunarizine, pizotifen and ethyl alcohol has been observed.

With simultaneous administration with ergotamine, a prolonged vasospasm was noted.

Sumatriptan can be prescribed no earlier than 24 hours after taking medications containing ergotamine; and vice versa, drugs containing ergotamine can be prescribed no earlier than 6 hours after taking sumatriptan.

Possible interaction between sumatriptan and MAO inhibitors, as well as sumatriptan and drugs from the group of selective serotonin reuptake inhibitors (SSRIs). There are separate reports on the development of weakness, hyperreflexia and coordination disorders in patients after taking sumatriptan and drugs from the SSRI group.In the case of simultaneous administration of sumatriptan and SSRIs, the patient's condition should be carefully monitored.

Special instructions:Sumatriptan should be prescribed only if the diagnosis of migraine is undoubted, and it should be used as soon as possible after the onset of a migraine attack, although it is equally effective when used at any stage of an attack.

Can not be used for preventive purposes.

As with the use of other antimigraine drugs, when prescribing sumatriptan in patients with a previously unidentified migraine or in patients with atypical migraine, other potentially serious neurologic conditions should be excluded. It should be noted that patients with migraine are at increased risk of developing certain cerebrovascular complications (stroke or transient cerebral circulation disorders).

Sumatriptan should not be prescribed to patients with suspected heart disease without a prior examination to exclude cardiovascular disease. Such patients include women in the postmenopausal period, men over the age of 40 and patients with risk factors for coronary heart disease.Although the examination does not always allow the identification of heart disease in some patients, in very rare cases they develop side effects from the cardiovascular system. After taking sumatriptan, transient intense pains and chest tightness that can spread to the neck area may occur.

If there is reason to believe that these symptoms are a manifestation of coronary heart disease, it is necessary to conduct an appropriate diagnostic examination.

Do not exceed the recommended dose of sumatriptan.

Effect on the ability to drive transp. cf. and fur:In patients with migraine, there may be drowsiness associated with both the disease itself and with the use of sumatriptan, so they should be especially careful when driving and working with moving mechanisms.

Form release / dosage:Tablets, film-coated, 50 mg and 100 mg.

Packaging:

By 2, 4, 6, 7 or 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

On 1, 2 contour acheikova packing with the instruction on application in a pack from a cardboard.

Storage conditions:

List B.In a dry, dark place at a temperature of not more than

25 ° C.

Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003235/09

Date of registration:27.04.2009 / 11.05.2012

Expiration Date:Unlimited

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp06.09.2015

Illustrated instructions

Instructions

Sumatriptan-OBL (Sumatriptan-OBL)