Eletriptan

被引:13
作者
Bardsley-Elliot, A [1 ]
Noble, S [1 ]
机构
[1] Adis Int Ltd, Auckland 10, New Zealand
关键词
D O I
10.2165/00023210-199912040-00006
中图分类号
R74 [神经病学与精神病学];
学科分类号
摘要
Eletriptan is a new serotonin 5-HT(1B/1D)receptor agonist developed for the treatment of acute migraine attacks. The increased lipophilicity of eletriptan provides ter absorption and improved oral bioavailability over that of sumatriptan. In animal studies, eletriptan effectively decreased carotid anastomotic blood flow, but exhibited a lower potential than sumatriptan to constrict coronary and femoral blood flow in a canine assay of potential adverse cardiovascular effects. Eletriptan was effective in reducing migraine pain from severe or moderate to mild or none within:! hours of administration of a single oral 40 or 80mg dose in a large, multicentre, double-blind placebo-controlled trial (n = 1151). In a double-blind, placebo-controlled comparative study, eletriptan (80mg, single oral dose) was significantly more effective than sumatriptan(100mg, single oral dose) in reducing headache pain at both 1 and 2 hours after administration (n = 692). Eletriptan is generally well tolerated. The most commonly reported adverse events were asthenia, somnolence, dizziness and nausea; these were typically mild and transient in nature.
引用
收藏
页码:325 / 333
页数:9
相关论文
共 37 条
[1]  
Bouchelet I, 1996, MOL PHARMACOL, V50, P219
[2]  
DOWSON A, 1998, 3 EFNS MIGR SEP 21, P4
[3]  
FARKKILA M, 1996, CEPHALALGIA, V16, P387
[4]  
GOADSBY PJ, 1999, IN PRESS NEUROLOGY
[5]   Characterisation of the contractile activity of eletriptan at the canine vascular 5-HT1B receptor [J].
Gupta, P ;
Scatchard, J ;
Napier, C ;
McHarg, A ;
Wallis, R .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1999, 367 (2-3) :283-290
[6]  
GUPTA P, 1997, HEADACHE, V37, P311
[7]  
Gupta P., 1996, CEPHALALGIA, V16, P386
[8]  
HAMEL E, 1993, MOL PHARMACOL, V44, P242
[9]  
HYLAND R, 1998, CEPHALALGIA, V18, P404
[10]  
JOHNSON BF, 1997, CEPHALALGIA, V17, P415