Active ingredient: Sumatriptan - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Vasoconstrictor Agents
• Selective Serotonin Agonists

Dosage Forms

• Tablet
• Injection
• Nasal spray

Brands / Synonyms

Alsuma; Imigran; Imitrex; Imitrex Injection; Imitrex Nasal; Sumatran; Sumatriptan; Sumatriptan Succinate; Sumatriptanum [Inn-Latin]; Sumavel Dosepro; Sumax ; Treximet

Indications

For the treatment of migraine attacks with or without aura in adults

Pharmacology

Sumatriptan, an antimigraine drug, is structurally similar to serotonin. It is thought that the cerebral blood vessel constriction induced by activation of 5-HT1 receptors on those vessels may contribute to the antimigrainous effect of sumatriptan in humans.

Mechanism of Action

Sumatriptan stimulates 5-HT receptors of the 1D subtype, most likely presynaptic receptors, resulting in selective vasoconstriction of inflamed and dilated cranial blood vessels in the carotid circulation. Sumatriptan also blocks the release of vasoactive neuropeptides from perivascular trigeminal axons in the dura mater during migraine and may inhibit the release of inflammatory mediators from the trigeminal nerve.

Absorption

~15%

Toxicity

convulsions, tremor, paralysis, inactivity, ptosis, erythema of the extremities, abnormal respiration, cyanosis, ataxia, mydriasis, salivation, and lacrimation; LD₅₀=mg/kg (orally in mice)

Biotrnasformation / Drug Metabolism

Hepatic. In vitro studies with human microsomes suggest that sumatriptan is metabolized by monoamine oxidase (MAO), predominantly the A isoenzyme.

Contraindications

Sumatriptan succinate tablets should not be given to patients with history, symptoms, or signs of ischemic cardiac, cerebrovascular, or peripheral vascular syndromes. In addition, patients with other significant underlying cardiovascular diseases should not receive sumatriptan succinate tablets. Ischemic cardiac syndromes include, but are not limited to, angina pectoris of any type (e.g., stable angina of effort and vasospastic forms of angina such as the Prinzmetal variant), all forms of myocardial infarction, and silent myocardial ischemia. Cerebrovascular syndromes include, but are not limited to, strokes of any type as well as transient ischemic attacks. Peripheral vascular disease includes, but is not limited to, ischemic bowel disease .

Because sumatriptan succinate tablets may increase blood pressure, they should not be given to patients with uncontrolled hypertension.

Concurrent administration of MAO-A inhibitors or use within 2 weeks of discontinuation of MAO-A inhibitor therapy is contraindicated (see CLINICAL PHARMACOLOGY, Drug Interactions and DRUG INTERACTIONS).

Sumatriptan succinate tablets should not be administered to patients with hemiplegic or basilar migraine.

Sumatriptan succinate tablets and any ergotamine-containing or ergot-type medication (like dihydroergotamine or methysergide) should not be used within 24 hours of each other, nor should sumatriptan succinate and another 5-HT₁ agonist.

Sumatriptan succinate tablets are contraindicated in patients with hypersensitivity to sumatriptan or any of their components.

Sumatriptan succinate tablets are contraindicated in patients with severe hepatic impairment.

Drug Interactions

Ergot-containing drugs have been reported to cause prolonged vasospastic reactions. Because there is a theoretical basis that these effects may be additive, use of ergotamine-containing or ergot-type medications (like dihydroergotamine or methysergide) and sumatriptan within 24 hours of each other should be avoided.

MAO-A inhibitors reduce sumatriptan clearance, significantly increasing systemic exposure. Therefore, the use of sumatriptan succinate tablets in patients receiving MAO-A inhibitors is contraindicated .

Selective serotonin reuptake inhibitors (SSRIs) (e.g., fluoxetine, fluvoxamine, paroxetine, sertraline) have been reported, rarely, to cause weakness, hyperreflexia, and incoordination when coadministered with sumatriptan. If concomitant treatment with sumatriptan and an SSRI is clinically warranted, appropriate observation of the patient is advised.