一种新型抗偏头痛药物阿莫曲坦的研究进展。

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Gras J, Llenas J, Jansat JM, Jauregui J, Cabarrocas X, Palacios JM

一种新型抗偏头痛药物阿莫曲坦的研究进展。

中枢神经系统药物，2002秋季刊;8(3):217-34。

PubMed ID

12353056 (PubMed视图

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摘要

阿莫曲坦是一种新型抗偏头痛药物，对人5-HT(1B)、5-HT(1D)和5-HT(1F)受体具有纳摩尔亲和力，对5-HT(1A)和5-HT(7)受体具有弱亲和力，对其他20多种药理受体无显著亲和力。阿莫曲坦在预测人类抗偏头痛活性的动物模型中是有效的，在动物研究中具有良好的安全性。从毒理学的角度来看，阿莫曲坦具有与其他已上市曲坦类药物相似的特性。在动物研究中，阿莫曲坦的水平大大高于人体治疗活性所需的水平，没有任何致癌、遗传毒性或致畸作用。阿莫曲坦口服吸收良好;它在人体中的绝对生物利用度为70%。给药后1 ~ 3小时达到血药峰值;其消除半衰期为3 ~ 4 h。阿莫曲坦代谢以单胺氧化酶介导的氧化脱氨和细胞色素p450介导的氧化为主要途径，黄素单加氧酶为次要途径。不需要根据性别或年龄调整剂量，只有在严重肾损害的情况下，24小时内剂量不应超过12.5 mg。单剂量阿莫曲坦与普萘洛尔、氟西汀或维拉帕米多剂量间无显著相互作用。 The efficacy of almotriptan in the treatment of acute migraine was demonstrated in clinical trials on more than 3000 patients with migraine. At two h after oral administration of almotriptan, 12.5 mg, the percentages of patients showing pain relief and a pain-free score were 64 and 36%, respectively. The effects of almotriptan were significantly better than those of placebo. When almotriptan was administered in the early phase of migraine, the percentage of pain-free patients at 2 h rose to 84%. In a phase III, double-blind and placebo-controlled study, the incidence of adverse events with almotriptan was not statistically different from that of placebo. Based on the available data, it appears that almotriptan is the triptan of choice when good efficacy and high tolerability are desired.

引用本文的药物库数据

药物酶

药物	酶	种类	生物	药理作用	行动
Almotriptan	胺氧化酶[含黄素	蛋白质	人类	未知的	底物	细节