Sumatriptan

Sumatriptan triptan) is an oral medication that can treat migraine and cluster headaches.This drug is an agonist of serotonin 5-HT1 receptors. The therapeutic effect of sumatriptan is apparently due to two mechanisms: the substance excites the serotonin 5-HT1 receptors of the smooth muscles of the carotid arterial system vessels and causes their narrowing. The carotid arteries supply blood to the tissues of the head, including meninges. In addition, sumatriptan activates the terminal receptors of afferent trigeminal fibers in the dura mater, resulting in decreased secretion of sensory neuropeptides. This medicine does not penetrate the BBB well and, according to the experimental data, does not possess painkillers proper. The effect of sumatriptan usually occurs 30 minutes after ingestion.

Indications

Migraine attacks with or without aura, including menstrual-associated migraines.

The drug is taken orally. The sooner you take the drug, the faster the healing effect occurs. Tablets should not be chewed or crushed somehow before swallowing.Adults take 1/2 tablet or a whole tablet. If the drug did not bring any therapeutic effect, then it is not recommended to take it again.

If the drug decreased or completely stopped pain, then it can be taken again within the next 24 hours.

The interval between taking the tablets should not be less than two hours. The maximum daily dose of sumatriptan should not exceed 300 mg.

Do not take these tablets if you have any of the following conditions:

• hypersensitivity to any of the components of the drug;
• lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
• hemiplegic, basilar and ophthalmoplegic forms of migraine;
• coronary heart disease (CHD), including angina pectoris (including Prinzmetal angina), myocardial infarction (including a history), post-infarction cardiosclerosis, as well as the symptoms suggesting the presence of CHD;
• occlusive peripheral vascular disease;
• a stroke or transient violation of cerebral circulation (including a history)
• uncontrolled arterial hypertension;
• simultaneous administration with drugs containing ergotamine or its derivatives (including methysergide), or other 5-HT receptors triptans/agonists;
• concomitant use with MAO inhibitors and a period of up to 14 days after discontinuation of these drugs;
• simultaneous administration with other agonists of 5-HT1-serotonin receptors;
• severe renal or hepatic insufficiency;
• age up to 18 years or older than 65 years (safety and efficacy of sumatriptan have not been established).

With caution: controlled arterial hypertension; diseases in which absorption, metabolism or excretion of sumatriptan (for example, impaired renal or hepatic function) may change; epilepsy (including any condition with a decrease in the threshold of convulsive readiness); hypersensitivity to sulfonamides (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 prescribing sumatriptan to such patients).

• Nervous system: dizziness, drowsiness, sensitivity disorders, including paresthesia and decreased sensitivity;
• Vessels: a transient increase in blood pressure (shortly after taking the drug), hot flashes;
• Respiratory system and chest organs: shortness of breath;
• Gastrointestinal tract: nausea, vomiting (a causal relationship between the occurrence of adverse reactions and administration the drug has not been proven);
• Musculoskeletal and connective tissue: a feeling of heaviness (usually transient, can be intense and occur in any part of the body, including the chest and throat), myalgia;
• General disorders and disorders at the injection site: pain, a feeling of cold or heat, a feeling of pressure or constriction (usually transient, can be intense and occur in any part of the body, including the chest and throat), weakness, fatigue (usually weak or moderate, transient);
• Laboratory and instrumental data: slight deviations in liver function tests.

No interaction of sumatriptan with propranolol, flunarizine, pizotifen and ethyl alcohol was noted.Concomitant use with ergotamine can cause a prolonged spasm of the vessels.

There is limited evidence of interaction with drugs containing ergotamine or other triptans/agonists of 5-HT serotonin receptors. This combination can theoretically increase the risk of coronary vasospasm, and the combined use of these drugs is contraindicated.

Sumatriptan can be used no earlier than 24 hours after taking drugs containing ergotamine, or other triptans/agonists of 5-N-serotonin receptors; and vice versa, preparations containing ergotamine can be used no earlier than 6 hours after taking sumatriptan; other triptans/agonists of 5-HTl-serotonin receptors can be used not earlier than 24 hours after taking sumatriptan.

Sumatriptan can interact with MAO inhibitors, their simultaneous use is contraindicated.

There are rare reports of the development of serotonin syndrome (including mental disorders, autonomic lability and neuromuscular disorders) resulting from the concomitant use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. Some patients also reported the development of serotonin syndrome after the simultaneous administration of triptans with selective serotonin and noradrenaline reuptake inhibitors (SSRIs). When they are used simultaneously, the patient’s condition should be carefully monitored.