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Eletriptan

Catalog No. DB00216 Name DrugBank
CAS Number 143322-58-1 Website http://www.ualberta.ca/
M. F. C22H26N2O2S Telephone (780) 492-3111
M. W. 382.51904 Fax (780) 492-1071
Purity Email david.wishart@ualberta.ca
Storage Chembase ID: 101

SYNONYMS

IUPAC name
5-[2-(benzenesulfonyl)ethyl]-3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-1H-indole
IUPAC Traditional name
relpax
Brand Name
Relpax
Synonyms
eletriptan

DATABASE IDS

CAS Number 143322-58-1
PubChem SID 46506380
PubChem CID 77993

PROPERTIES

Hydrophobicity(logP) 3.9
Solubility Readily soluble as hydrobromide formulation

DETAILS

Description (English)
Item Information
Drug Groups approved; investigational
Description Eletriptan is a second generation triptan drug developed by Pfizer Inc for the treatment of migraine headaches. [Wikipedia]
Indication For the acute treatment of migraine with or without aura in adults.
Pharmacology 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 observed. Eletriptan has also been shown to inhibit trigeminal nerve activity in the rat.
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
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.
Absorption Well absorbed after oral administration with a mean absolute bioavailability of approximately 50%.
Half Life The terminal elimination half-life of eletriptan is approximately 4 hours.
Protein Binding Plasma protein binding is moderate and approximately 85%.
Distribution * 138 L
Clearance * Renal cl=3.9 L/h
External Links
Wikipedia
RxList
PDRhealth
Drugs.com

REFERENCES