Almotriptan,一个新的anti-migraine代理:审查。

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肝J, llena J, Jansat JM,哈乌雷吉曾J, Cabarrocas X,帕拉西奥斯JM

Almotriptan,一个新的anti-migraine代理:审查。

中枢神经系统药物启2002下降;8 (3):217 - 34。

PubMed ID

12353056 (在PubMed

]

文摘

Almotriptan是人类的新anti-migraine剂摩尔亲和力5 - (1 b), 5 - (1 d)和5(1)受体,弱亲和力5 - (1 a)和5(7)受体和无显著关联的其他20多位药理受体。Almotriptan anti-migraine活动是有效的在动物模型预测人类和动物研究有很好的安全性。从毒理学的角度来看,almotriptan剖面类似于其他市场的药物。在动物实验中,水平大大高于在人类所需的治疗活动,almotriptan是没有任何致癌基因毒性或致畸效应。Almotriptan是口服吸收;它在人类的绝对生物利用度为70%。等离子体水平达到了自己的巅峰1到3小时后管理;它的消除半衰期是3到4 h。Almotriptan由单胺代谢oxidase-mediated氧化脱氨基作用和细胞色素P450-mediated氧化的主要代谢途径和黄素单氧酶作为次要的路线。不需要剂量调整性别或年龄,且仅在严重肾功能损害的剂量在24小时内不应超过12.5毫克。没有明显almotriptan一剂之间的相互作用和普萘洛尔,氟西汀或维拉帕米,在多个剂量。 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.

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药物酶

药物	酶	类	生物	药理作用	行动
Almotriptan	胺氧化酶(flavin-containing)	蛋白质	人类	未知的	底物	细节