| Item |
Information |
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Drug Groups
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approved; investigational |
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Description
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A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of migraine disorders. A transdermal patch version of sumatriptan is currently in phase I trials in the U.S. under the code name NP101 (NuPathe). |
| 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 alpha1-, alpha2-, or beta-adrenergic; dopamine1; dopamine2; muscarinic; or benzodiazepine receptors. |
| 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 |
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| Biotransformation |
Hepatic. In vitro studies with human microsomes suggest that sumatriptan is metabolized by monoamine oxidase (MAO), predominantly the A isoenzyme. |
| Absorption |
Approximately 15% |
| Half Life |
2.5 hours |
| Protein Binding |
14%-21% |
| 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. |
| Distribution |
* 2.7 L/kg [subcutaneous dosing] |
| Clearance |
* 1200 mL/min [Following a 6-mg SC injection] |
| References |
| • |
Nikai T, Basbaum AI, Ahn AH: Profound reduction of somatic and visceral pain in mice by intrathecal administration of the anti-migraine drug, sumatriptan. Pain. 2008 Oct 31;139(3):533-40. Epub 2008 Aug 23.
[Pubmed]
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| External Links |
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