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QuickView for Eletriptan (compound)

Name: eletriptan
PubChem Compound ID: 156849
Molecular formula: C22H27BrN2O2S
Molecular weight: 463.432 g/mol
Relpax; 177834-92-3; Eletriptan Hydrobromide [USAN]; UK 116044-04; Eletriptan hydrobromide; 1H-Indole, 3-(((2R)-1-methyl-2-pyrrolidinyl))methyl)-5-(2-(phenylsulfonyl)ethyl)-, monohydrobromide
Name: eletriptan
Name (isomeric): DB00216
Drug Type: small molecule
Brand: Relpax
Category: Serotonin Agonists, Selective Serotonin Agonists, Vasoconstrictor Agents, Anti-migraine Agents, Anti-inflammatory Agents
CAS number: 143322-58-1
Indication: For the acute treatment of migraine with or without aura in adults.
Eletriptan is a selective 5-hydroxytryptamine 1B/1D receptor agonist. In the anesthetized dog, eletriptan has been shown to reduce carotid arterial blood flow, with only a small increase in arterial blood pressure at high doses. While the effect on blood flow was selective for the carotid arterial bed, decreases in coronary artery diameter were obs...
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Mechanism of Action:
Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors, and little or no affinity for 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, 5-HT5A and 5-HT6 receptors. Eletriptan has no significant affinity or pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic...
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Absorption: Well absorbed after oral administration with a mean absolute bioavailability of approximately 50%.
Protein binding: Plasma protein binding is moderate and approximately 85%.
Biotransformation: In vitro studies indicate that eletriptan is primarily metabolized by cytochrome P-450 enzyme CYP3A4. The N-demethylated metabolite of eletriptan is the only known active metabolite.
Half Life: The terminal elimination half-life of eletriptan is approximately 4 hours.
Clearance: Renal cl=3.9 L/h
Toxicity: Based on the pharmacology of the 5-HT1B/1D agonists, hypertension or other more serious cardiovascular symptoms could occur on overdose.
Affected organisms: Humans and other mammals
Food interaction:
Exposure to the product (area below curve) and maximum concentrations are increased when product is taken with a high-fat meal.
Drug interaction:
ErgotaminePossible severe and prolonged vasoconstriction
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of eletriptan by decreasing its metabolism. Consider avoiding administration of the two agents within 72 hours of each other. Monitor for changes in the therapeutic and adverse effects of eletriptan if voriconazole is initiated, discontinued or dose changed.
FluvoxamineIncreased risk of CNS adverse effects
TramadolIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
TroleandomycinThe macrolide, troleandomycin, may increase the effect and toxicity of eletriptan.
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