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福瑞他滨的药代动力学评估。

Pharmacokinetic evaluation of frovatriptan.

机构信息

Sapienza University, Regional Referral Headache Center, School of Health Sciences, Department of Medical and Molecular Sciences, Rome, Italy.

出版信息

Expert Opin Drug Metab Toxicol. 2011 Nov;7(11):1449-58. doi: 10.1517/17425255.2011.622265. Epub 2011 Sep 20.

Abstract

INTRODUCTION

Migraine is the most common painful neurological disorder, affecting 13% of the general population. Triptans represent a powerful pharmacological tool in acute migraine treatment, however, a significant portion of treated patients cannot have access to this class due to possible adverse affects. Today, a total of seven triptan molecules are available, representing a commonly prescribed migraine treatment. Although there is a need of extensive use of triptans, only 25% of migraine patients are using triptans.

AREAS COVERED

This review includes triptans and evidence for the use of frovatriptan. A systematic approach is used to discuss the pharmacodynamic and pharmacokinetic aspects of frovatriptan, considering the emerging data on the clinical efficacy of frovatriptan in the treatment of migraine and cluster headaches. The data were obtained by searching the following key words in MEDLINE: pharmacokinetic, pharmacodynamic, triptans, frovatriptan, migraine, menstrual migraine, relatively to the period 1988 - 2011.

EXPERT OPINION

Frovatriptan has been developed in order to improve safety and efficacy of triptans. It shows a favorable tolerability and efficacy profile, limited to 24/48-h headache recurrence, when compared with other triptans. Preclinical data suggest that the pharmacokinetic profile of frovatriptan may differ from other available triptans. In fact, among triptans, frovatriptan showed the highest potency at the 5-HT1B receptor (8.2) and the longer half-life (26 h). These parameters determine the clinical properties of frovatriptan; in particular the lowest rate of headache recurrence in comparison with other triptans.

摘要

简介

偏头痛是最常见的疼痛性神经疾病,影响 13%的普通人群。曲普坦类药物是治疗急性偏头痛的有力药物,但由于可能的不良反应,相当一部分患者无法使用此类药物。目前,共有七种曲普坦类药物可供使用,是治疗偏头痛的常用药物。尽管曲普坦类药物的使用需求广泛,但只有 25%的偏头痛患者在使用曲普坦类药物。

涵盖领域

本文综述了曲普坦类药物和氟伐曲坦的应用证据。本文采用系统的方法讨论了氟伐曲坦的药效学和药代动力学特征,同时考虑了氟伐曲坦在治疗偏头痛和丛集性头痛方面的临床疗效的新数据。数据通过在 MEDLINE 中搜索以下关键词获得:药代动力学、药效学、曲普坦类、氟伐曲坦、偏头痛、经期偏头痛,检索时间范围为 1988 年至 2011 年。

专家意见

氟伐曲坦的开发旨在提高曲普坦类药物的安全性和疗效。与其他曲普坦类药物相比,氟伐曲坦具有良好的耐受性和疗效,头痛复发率限制在 24/48 小时内。临床前数据表明,氟伐曲坦的药代动力学特征可能与其他可用的曲普坦类药物不同。事实上,在曲普坦类药物中,氟伐曲坦对 5-HT1B 受体的亲和力最高(8.2),半衰期最长(26 小时)。这些参数决定了氟伐曲坦的临床特性;特别是与其他曲普坦类药物相比,头痛复发率最低。

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