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QuickView for sumatriptan (compound)


PubChem
Name: Sumatriptan
PubChem Compound ID: 10613956
Description: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.
Molecular formula: C14H21N3O2S
Molecular weight: 297.394 g/mol
DrugBank
Identification
Name: Sumatriptan
Name (isomeric): DB00669
Drug Type: small molecule
Description: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.
Synonyms:
NP101; Sumatriptan Succinate; triptan; Sumatriptanum [INN-Latin]
Brand: Sumax, Sumatran, Imigran, Imitrex Oral, Imitrex
Category: Serotonin Agonists, Selective Serotonin Agonists, Vasoconstrictor Agents
CAS number: 103628-46-2
Pharmacology
Indication: For the treatment of migraine attacks with or without aura.
Pharmacology:
Sumatriptan, an antimigraine drug, is a selective agonist of vascular serotonin ((5-hydroxytryptamine; 5-HT) type 1-like receptors, likely the 5-HT1D and 5-HT1B subtypes. It has no significant affinity (as measured using standard radioligand binding assays) or pharmacological activity at 5-HT2, 5-HT3 receptor subtypes or at al...
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Mechanism of Action:
The 5-HT1B and 5-HT1D receptors function as autoreceptors, which inhibit the firing of serotonin neurons and a reduction in the synthesis and release of serotonin upon activation. After sumatriptan binds to these receptors, adenylate cyclase activity is inhibited via regulatory G proteins, incrases intracellular calcium, and a...
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Absorption: Approximately 15%
Protein binding: 14%-21%
Biotransformation: Hepatic. In vitro studies with human microsomes suggest that sumatriptan is metabolized by monoamine oxidase (MAO), predominantly the A isoenzyme.
Route of elimination: Only 3% of the dose is excreted in the urine as unchanged sumatriptan; 42% of the dose is excreted as the major metabolite, the indole acetic acid analogue of sumatriptan.
Half Life: 2.5 hours
Clearance: 1200 mL/min [Following a 6-mg SC injection]
Toxicity: Symptoms of overdose include convulsions, tremor, paralysis, inactivity, ptosis, erythema of the extremities, abnormal respiration, cyanosis, ataxia, mydriasis, salivation, and lacrimation.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
ErgotaminePossible severe and prolonged vasoconstriction
FluvoxamineIncreased risk of CNS adverse effects
TramadolIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
VilazodoneIncreased risk of serotonin syndrome
TrimipramineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
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