Name: | Sumatriptan |
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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 |
Name: | Sumatriptan |
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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]
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Brand: | Sumax, Sumatran, Imigran, Imitrex Oral, Imitrex |
Category: | Serotonin Agonists, Selective Serotonin Agonists, Vasoconstrictor Agents |
CAS number: | 103628-46-2 |
Indication: | For the treatment of migraine attacks with or without aura. |
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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 |
Drug interaction: |
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