Thomas Jefferson University Hospitals, Wayne, Pennsylvania, USA.
Drugs Today (Barc). 2021 Feb;57(2):89-100. doi: 10.1358/dot.2021.57.2.3238326.
Lasmiditan, a selective 5-HT1F receptor agonist, is a harbinger for the novel ditan class of medications for acute migraine treatment. Lasmiditan activates 5-HT1F receptors on presynaptic trigeminal nerve terminals, which impedes the release of calcitonin gene-related peptide (CGRP) from trigeminal nerve endings and thereby suppresses activation of the trigeminovascular system. Notably, lasmiditan does not result in vasoconstriction, making lasmiditan a migraine-specific acute treatment option for those with cardiovascular risk factors. However, lasmiditan does have centrally mediated side effects. This review will discuss the background of lasmiditan development, its preclinical pharmacology, safety, drug interactions and indications for use.
拉米地坦是一种选择性 5-HT1F 受体激动剂,是新型坦类药物治疗急性偏头痛的先驱。拉米地坦激活三叉神经末梢突触前 5-HT1F 受体,阻止降钙素基因相关肽(CGRP)从三叉神经末梢释放,从而抑制三叉血管系统的激活。值得注意的是,拉米地坦不会导致血管收缩,使拉米地坦成为有心血管危险因素的偏头痛患者的特异性急性治疗选择。然而,拉米地坦确实有中枢介导的副作用。本文将讨论拉米地坦的开发背景、临床前药理学、安全性、药物相互作用和适应证。