Sumatriptan

Brand Canonpharma

In stock 1498 Items

Available since: 2019-09-19

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Clinical Pharmacology

Pharmacotherapeutic group: an anti-migraine agent.

KODATH: [N02CC01]

Pharmacodynamics

Antifungal agent. A specific and selective agonist of 5-HT1-serotonin receptors, localized predominantly in the blood vessels of the brain, and has no effect on other subtypes of 5-HT-serotonin receptors (5-HT2-7). Causes vasoconstriction of the carotid arterial bed, which supply blood to extracranial and intracranial tissues (dilation of the meninges and / or their edema is the main mechanism of migraine development in humans), without having a significant effect on 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 migraine attack. In 50–70% of cases, it quickly eliminates a seizure when taken orally at a dose of 25–100 mg. Within 24 hours, 1/3 of cases may develop a relapse, requiring repeated use.

Onset of action - 30 minutes after ingestion in a dose of 100 mg.

Pharmacokinetics

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

Communication with plasma proteins - 14–21%, total volume of distribution - 170 l (2.4 l / kg).

It is metabolized by oxidation with the participation of monoamine oxidase (MAO) (mainly isoenzyme A) to form metabolites, the main of which are the indole-analogue of sumatriptan, which does not have pharmacological activity against 5-НТ1- and 5-НТ2-serotonin receptors, and its glucuronide.

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

Indications

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

Composition

Composition: 1 tablet, film coated, contains:

sumatriptan succinate active ingredient 70 mg and 140 mg. in terms of sumatriptan 50 mg and 100 mg;

excipients: hyprolosis (hydrocate and propyl cellulose Klucel LF, calcium hydrophosphate dihydrate, mannitol (mannitol). magnesium stearate. croscarmellose sodium (primelloza), microcrystalline cellulose;

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

Sumatriptan is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Sumatriptan	Canonpharma	Russia	pills
Amigrenin	Veropharm	Russia	pills
Sumatriptan	Vertex	Russia	pills
Sumatriptan-Teva	Teva	Israel	pills
Sumatriptan	Berezovsky Pharmaceutical Plant	Russia	pills
Sumatriptan-OBL	Obolensky OP	Russia	pills
Sumamigren	Polpharma	Poland	pills

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Dosage and Administration

Sumatriptan is not intended for prophylactic use.

Adults are prescribed in a single dose of 50 mg, in some cases - 100 mg. The maximum daily dose is 300 mg.

If the symptoms of migraine do not disappear and do not decrease after taking the first dose of Sumatriptan, then the drug should not be prescribed again to relieve an ongoing attack. If the symptoms have decreased or disappeared, and then resumed, a second dose can be taken in the next 24 hours. The interval between doses of the drug should be at least 2 hours.

Adverse reactions

Cardiovascular system: hyperemia of the skin and mucous membranes, arterial hypotension, tachycardia, palpitations, angina, transient increase in blood pressure, transient changes of ischemic type ECG, bradycardia; in isolated cases - manifestations of Raynaud's syndrome.

CNS: dizziness, weakness, drowsiness, feeling tired; visual impairment (diplopia, scotoma, reduced visual acuity).

On the part of the digestive system: a feeling of discomfort in the abdomen, dysphagia, nausea, vomiting; rarely - ischemic colitis, increased activity of liver enzymes.

Allergic reactions: rash, pruritus, erythema, urticaria, anaphylaxis.

Other: possible tingling, warmth, heaviness, pressure or compression in different parts of the body, myalgia.

Contraindications

- hemiplegic, basilar and ophthalmoplegic forms of migraine;

- IHD (including angina);

- occlusive peripheral arterial disease;

- uncontrolled arterial hypertension;

- stroke or transient cerebral circulation (including in history);

- severe liver dysfunction;

- simultaneous administration of preparations containing ergotamine or its derivatives;

- simultaneous administration of MAO inhibitors and a period of up to 14 days after their cancellation;

- pregnancy;

- lactation period (breastfeeding);

- The age of patients under 18 and over 65;

- Hypersensitivity to the drug.

Drug interactions

When taken concomitantly with ergotamine, prolonged vasospasm was observed. Sumatriptan can be prescribed no earlier than 24 hours after taking medications containing ergotamine.

Interaction between sumatriptan and MAO inhibitors is possible, their simultaneous use is contraindicated.

There are separate reports of the development of weakness, hyperreflexia and impaired coordination in patients after simultaneous administration of sumatriptan and selective serotonin reuptake inhibitors. Do not simultaneously appoint Sumatriptan and drugs in this group.

Do not simultaneously appoint Sumatriptan and lithium preparations

Pregnancy and Lactation

The drug is contraindicated for use during pregnancy and lactation (breastfeeding).

Special instructions

With extreme caution, sumatriptan should be prescribed for epilepsy (including in any conditions with a decrease in seizure threshold), as well as in patients with controlled arterial hypertension.

When Sumatriptan is prescribed to patients with newly diagnosed migraine or with migraine that occurs with atypical symptoms, other potentially dangerous neurological diseases should be excluded. It must be borne in mind that in patients with migraine there is a risk of cerebrovascular complications (including stroke or transient cerebral circulatory disorders).

The drug should not be prescribed to patients at risk of developing the pathology of the cardiovascular system, without prior examination to exclude the disease. The first 2-3 doses of the drug should be carried out under medical supervision (as a spasm of the coronary arteries is possible).

In patients with hypersensitivity to sulfonamides when taking sumatriptan may develop allergic reactions that range from skin manifestations to anaphylactic shock.

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

Clinical experience with the drug in patients over the age of 65 years is limited (there is no significant difference in pharmacokinetics compared with younger patients).

Influence on ability to drive motor transport and control mechanisms

With sumatriptan therapy, drowsiness may develop. Therefore, during the period of use of the drug, patients should be extremely careful to drive a car and engage in other potentially dangerous activities that require high-speed psychomotor reactions.