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%.
An N-alkylpyrrolidine, that is N-methylpyrrolidine in which the pro-R hydrogen at position 2 is replaced by a {5-[2-(phenylsulfonyl)ethyl]-1H-indol-3-yl}methyl group.
参考文献
PubChem文献
数据源提供
• Goadsby, P.J., et al.: Neurology, 54, 156 (2000)
• Willems, E., et al.: Arch. Pharmacol., 358, 212 (1998)
• Napier, C., et al.: Eur. J. Pharmacol., 368, 259 (1998)
