抗偏头痛新药洛美利嗪

Lomerizine,a new antimigraine agent

洛美利嗪 ,一种新型二苯哌嗪类衍生物 ,目前临床上主要治疗偏头痛和丛集性头痛。洛美利嗪与氟桂利嗪等钙通道拮抗剂不同 ,具有钙通道和钠通道双重阻断作用 ,洛美利嗪在nmol·L-1至 μmol·L-1水平 ,在多部位具有生物活性 ,包括血管和神经元钙通道、钠通道、α1肾上腺素受体和 5 HT2 受体 ,以及自由基清除作用。本文综述了洛美利嗪的药理作用、药动学与临床疗效等。

Lomerizine,a new calcium antagonist of the diphenylpiperazine type,is mainly used for the treatment of migraine and cluster headache. Lomerizine acts as dual sodium and calcium channel blocker. It has high nmol·L -1 to μmol·L -1 activity at multiple sites, including both vascular and neuronal calcium channels, sodium channel,α 1 adrenoceptors and 5-HT 2 receptors,as well as a free radical scavenger.This review summarizes the structure-action relation,pharmacodynamics,pharmacokinetics,clinical uses and safty of lomerizine.