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依立曲坦

Eletriptan.

作者信息

Gawel M J, Grujich N N

机构信息

Division of Neurology, Sunnybrook & Women's College Health Sciences Centre, University of Toronto, Toronto, ON, Canada.

出版信息

Expert Opin Investig Drugs. 2001 Oct;10(10):1869-74. doi: 10.1517/13543784.10.10.1869.

Abstract

Eletriptan (Relpax, Pfizer) is one of a group of anti-migraine medications commonly referred to as 'triptans'. It is a potent serotonin agonist at the 5-HT(1B/1D) receptor and is indicated for the acute treatment of migraine headaches. Eletriptan is administered orally. It is rapidly absorbed and has a bioavailability of 50% compared to 14% for sumatriptan. The relatively high lipophilicity of eletriptan compared to sumatriptan may explain its faster oral absorption and shorter time to onset of action. Results from comparative studies between oral eletriptan and sumatriptan indicate that eletriptan 80 mg was superior to sumatriptan 100 mg in onset of action, headache response rate, pain free response rate and relief of associated migraine symptoms at the 1 or 2 h time intervals. Although there was a modest increase in adverse events with eletriptan 80 mg than with sumatriptan 100 mg, eletriptan received a high patient acceptability rating (84%).

摘要

依立曲坦(Relpax,辉瑞公司)是一类通常被称为“曲坦类”的抗偏头痛药物之一。它是一种强效的5-HT(1B/1D)受体血清素激动剂,用于偏头痛的急性治疗。依立曲坦通过口服给药。它吸收迅速,生物利用度为50%,而舒马曲坦为14%。与舒马曲坦相比,依立曲坦相对较高的亲脂性可能解释了其更快的口服吸收和更短的起效时间。口服依立曲坦和舒马曲坦的对比研究结果表明,在1或2小时的时间间隔内,80毫克依立曲坦在起效、头痛缓解率、无痛缓解率和相关偏头痛症状缓解方面优于100毫克舒马曲坦。尽管80毫克依立曲坦的不良事件比100毫克舒马曲坦略有增加,但依立曲坦获得了较高的患者接受度评分(84%)。

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