Brands, Medical Use, Clinical Data
- Vasoconstrictor Agents
- Selective Serotonin Agonists
- Nasal spray
Brands / Synonyms
Alsuma; Imigran; Imitrex; Imitrex Injection; Imitrex Nasal; Sumatran; Sumatriptan; Sumatriptan Succinate; Sumatriptanum [Inn-Latin]; Sumavel Dosepro; Sumax
For the treatment of migraine attacks with or without aura in adults
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.
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.
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
Sumatriptan succinate tablets should not be administered to patients with hemiplegic or basilar
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.
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.