Sumatriptan

Sumatriptan is a drug with antimigraine activity.

The active substance of the sumatriptan tablets has a stimulating effect on the 5-HT1 receptors of the predominantly blood vessels of the membranes and brain substances. Due to this influence, narrowing of locally dilated vessels occurs, due to which the pain intensity decreases during the development of the migraine attack. The drug has no direct analgesic effect, therefore it is not an analgesic.

The drug can effectively suppress migraine attacks already with a single application in a dose of up to 100 mg. Sumatriptan begins to act after a maximum of half an hour from the time it is ingested.

Clinical and pharmacological group

The agonist of serotonin 5-HT1 receptors. The drug with antimigraine activity.

Terms of sale from pharmacies

Can buyby prescription.

Price

How much does sumatriptan cost in pharmacies? The average price is at the level of120 rubles.

Composition and form of release

Medicinal forms of the release of sumatriptan:

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• tablets covered with a film sheath: biconvex, round, white (2, 6 or 10 pcs. in blisters, in a cardboard bundle of 1-3 blisters);
• tablets: oblong, biconcave, almost white or white, on one side engraving "C", on the other (depending on the dose) - "33" (50 mg) or "34" (100 mg) (1-7 or 10 PC. in blisters, in a cardboard bundle 1-6, 8 or 10 blisters; by 2, 10, 50 or 100 pieces. in banks, in a cardboard bundle of 1 bank).

Composition of 1 film-coated tablets:

• active substance: sumatriptan - 50 or 100 mg (sumatriptan succinate - 70 or 140 mg);
• auxiliary components (50/100 mg): croscarmellose sodium - 2/4 mg; talc - , / 3 mg; magnesium stearate - , / 3 mg; lactose monohydrate - 125/250 mg; microcrystalline cellulose - 100/200 mg;
• Sheath (50/100 mg): polysorbate-80 - 0.88 / 1.76 mg; titanium dioxide - 0.92 / 1.84 mg; hypromellose - 5.9 / 11.8 mg; macrogol 6000 - 2.3 / 4.6 mg.

Composition of 1 tablet:

• active substance: sumatriptan - 50 or 100 mg (in the form of sumatriptan succinate - 69.98 or 139.96 mg);
• auxiliary components (50/100 mg): magnesium stearate - 2.38 / 4.76 mg; sodium hydrogencarbonate - 10/20 mg; calcium hydrogen phosphate - 53.44 / 106.88 mg; croscarmellose sodium - 11/22 mg; microcrystalline cellulose - 22.5 / 45 mg; polysorbate-80 - 0.7 / 1.4 mg.

pharmachologic effect

The active component of the drug is a specific selective agonist of 5-HT1-serotonin receptors, which are concentrated mainly in the vessels of the brain. Some subtypes of serotonin receptors fall under its influence. An example is 5-HT 2-7. As a result, the vessels of the arterial bed narrow. Their expansion is the cause of edema and the subsequent occurrence of migraine.

The effect is manifested after half an hour after ingestion of the tablet inside. Pharmacokinetics of the drug:

• metabolized by oxidation with the participation of monoamine oxidase to form metabolites - indoleuxide analogue sumatriptan and its glucuronide;
• is excreted by the kidneys in the form of metabolites;
• quickly absorbed after ingestion, reaching 70% of the maximum concentration after 45 minutes;
• bioavailability is 14% due to incomplete absorption and presystemic metabolism;
• the maximum concentration in the blood plasma is 54 ng / ml;
• binding to blood proteins is 14-21%;
• the half-life is 2 hours;
• in patients with impaired liver function, the plasma content of the active component in the blood increases.

The drug reduces the isolation of sensory neuropeptides by suppressing the excessive activity of the trigeminal nerve receptors. Against this background, there is no significant effect on the blood flow in the brain. The result is the elimination of nausea, photophobia and other migraine symptoms. This requires a single dose of 100 mg.

Indications for use

The drug compound is recommended for use in migraines for relief of acute attacks of the disease and further stabilization of the condition.

Contraindications

In the presence of any deviations, it is strictly forbidden to take "Sumatriptan" medication, analogues of this drug? I would like to especially note that the instruction contains a lot of information on this matter. That is why before taking the drug with it should be sure to read.

So what contraindications does the presented drug have? Let's consider the list right now:

• angina pectoris, including angina of Prinzmetal;
• pregnancy and breastfeeding;
• myocardial infarction, including those taking place in the anamnesis;
• arterial hypertension (uncontrolled type);
• arterial hypertension (controlled type);
• increased sensitivity of the patient to the elements of the drug;
• elderly patient (over 65 years old);
• basilar, ophthalmoplegic or hemiplegic form of migraine;
• simultaneous reception of a medicinal product with medicines that contain ergotamine, its various derivatives, as well as MAO inhibitors (it is forbidden to take the drug for up to 14 days after the abolition of the mentioned drugs);
• ischemic heart disease, as well as a suspicion of it;
• teenage and children's age (up to 18 years);
• Occlusal diseases of peripheral arteries;
• epilepsy, including any pathological conditions associated with a reduced epileptic threshold;
• renal or hepatic impairment;
• stroke, or a transient condition of cerebral circulation, including those that occur in the anamnesis.

As mentioned above, the drug "Sumatriptan" during pregnancy is prohibited. But if the risk to the fetus is less than the benefit to the mother, then it is still prescribed to women in the position and nursing mothers. However, only an experienced specialist should do this (the drug is taken strictly under his supervision). By the way, it is extremely not recommended to breastfeed a baby within 24 hours after taking these pills.

Intended use for pregnancy and lactation

Sumatriptan is contraindicated in pregnancy. It is not recommended to continue breastfeeding within 24 hours after using the medication.

Dosage and route of administration

As indicated in the instructions for use, sumatriptan is administered orally, the tablet should be swallowed whole, with water. Begin treatment as soon as possible in the event of a migraine attack. The recommended dose is 50 mg, if necessary 100 mg.

• If migraine symptoms do not disappear and do not decrease after taking the first dose, then the drug is not used again to stop the same attack.

To stop subsequent seizures (with a decrease or disappearance of symptoms, and then resume), you can take the second dose within the next 24 hours, provided that the interval between taking is at least 2 hours.

The maximum daily dose is 300 mg.

Side effect

Against the background of the use of tablets, Sumatriptan may develop negative pathological reactions from various organs and systems:

• Organs of feelings - double vision (diplopia), reduced visual acuity, the appearance of "flies" before the eyes.
• Respiratory system - non-expressed irritation of the mucous membrane of the nasal cavity, accompanied by burning, respiratory failure (dyspnea), development of nasal bleeding.
• Cardiovascular system - a transient increase in the level of systemic arterial pressure (arterial hypertension), which usually normalizes after drug withdrawal, "hot flashes" with a feeling of heat in the face, heart rhythm disturbance (arrhythmia), palpitations (tachycardia).
• Nervous system - drowsiness, dizziness, violation of skin sensitivity, characterized mainly by its decrease (paresthesia), sensation of cold or heat in the skin, having different localization, general weakness, increased fatigue, it is rare to develop epileptic seizures accompanied by convulsions.
• Musculoskeletal system - a sudden appearance of a feeling of heaviness or squeezing in any part of the body, it is often localized in the chest, has a transient nature.
• The digestive system - nausea, accompanied by vomiting, deviations in the level of liver enzymes of the blood, indicating an increased strain on the organ with damage its cells, discomfort in the abdomen, ischemic colitis (inflammation of the large intestine, which develops as a result of circulatory disturbances in its walls).
• Allergic reactions - a rash on the skin, its itching, severe systemic reactions like anaphylactic shock (a critical decrease in the level of systemic arterial pressure with multiple organ failure).

When negative pathological reactions occur against the background of the use of this medication, they are usually discarded or adjusted dosage

Overdose

The development of any other adverse reactions other than those mentioned above, when taking a dose of 400 mg is not observed.

In case of an overdose, for a minimum of 10 hours, the patient's condition should be monitored, and support treatment if necessary. Information on the effect of peritoneal dialysis / hemodialysis on the plasma concentration of sumatriptan is absent.

special instructions

Do not use to prevent a migraine attack.

During the treatment period, care must be taken when driving a motor vehicle and doing other activities. potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Patients at risk of cardiovascular disease do not start therapy without a preliminary examination (women in the postmenopausal period, men over the age of 40, persons with risk factors for the development of IHD). Before prescribing sumatriptan to patients with a newly diagnosed or atypical migraine, other potentially neurological diseases should be excluded. After taking sumatriptan, pain and a feeling of tightness in the chest may occur. The pain can be intense and radiate into the neck. If there is reason to believe that these symptoms are a manifestation of CHD, it is necessary to conduct an appropriate examination.

Interaction with other drugs

No interaction of sumatriptan with propranolol, flunyrizine, pizotifen and ethanol has been observed.

With the simultaneous administration of ergotamine and ergotamine-containing drugs, a prolonged vasospasm is possible.

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

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

Reviews

We offer you to read reviews of people who used the drug Sumatriptan:

1. Elena. Yes, they help, but very strong side effects. Absence of concentration, drowsiness such that from the bed I can not get up all day. After they are hired, you can not walk, there is no point. I'll look for another way out, I'm sick with them and the pain the next day began to return. Be healthy!
2. Marina. According to a doctor's prescription I buy tablets with a dosage of 50 mg. It helps well, most importantly - quickly. Side effects sometimes arise, but in comparison with migraine pain they do not equal. The price for 2 tablets is low - about 130 rubles, but sometimes I need much more, so it goes a little expensive. In general, I recommend this medicine.
3. Tamara. It is only this drug that helps. And the fact that he made a prescription just kills. I wish the authors of this order themselves to suffer from migraines. If the attack is overtaken and there is no pill, then you go out of order for two or three days. And also in a polyclinic to be dragged behind the prescription it simply behind a side of goods and harm. Where can you even complain about these "lawmakers"?

Analogues

Tablets from migraine sumatriptan have several analogs. They are divided into 2 categories. The first is similar to this drug in composition, and the second - according to the principle of action. Among the popular analogues are:

1. Sumatriptan-Teva. Is only available in a dosage of 50 mg. In other respects, the preparation has practically no difference.
2. Rapimed. It is based on the same substance. The difference between this medication is that the peak concentration of the drug occurs at a time 2-2.5 hours after ingestion. The medicine is excreted from the body longer - for 2.5 hours.
3. Amigrenin. Used for migraine with or without aura. Instructions for use are similar. With caution, this drug is used for arterial hypertension and epilepsy.
4. Sumygamren. It is based on the same active component, shows a similar principle of action, therefore it is a complete analogue of this drug.

Before buying an analogue, consult your doctor.

Shelf life and storage conditions

Store in a dry, protected from light, out of reach of children place at a temperature of 15 0 C to 25 0 C.

Shelf life - 2 years.

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