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Drugs targeting 5-hydroxytryptamine receptors in acute treatments of migraine attacks. A review of new drugs and new administration forms of established drugs

机译:在偏头痛发作的急性治疗中靶向5-羟色胺受体的药物。审查新药和现有药物的新管理形式

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Introduction: The development of sumatriptan, more than 20 years ago, added substantially to the characterization of 5-hydroxytryptamine (5-HT) receptors and their relevance to acute migraine therapy. Recently, 5-HT1F receptor agonists, with no vascular effects, have shown efficacy in the treatment of migraines. Areas covered: This evaluation reviews the recent advances in acute migraine therapy targeting the 5-HT receptor. Specifically, the authors review the pharmacokinetics, pharmacodynamics, clinical efficacy and safety of 5-HT1F receptor agonists and new formulations of sumatriptan and dihydroergotamine (DHE). Expert opinion: Lasmiditan, a non-vascular acting 5-HT1F receptor agonist, is effective in migraine but causes central nervous system-related adverse events, which may considerably limit its clinical use. The efficacy of transdermal sumatriptan is too low for general use in migraine. Intranasal sumatriptan powder could be a step forward compared with oral sumatriptan, but comparative trials are needed. Orally inhaled DHE has a very quick systemic absorption but the onset of effect in migraine is relatively slow with a maximum effect after 2 h. In contrast, orally inhaled DHE results in a low incidence of recurrence. None of these reviewed treatments are likely to fulfill patients' expectations, and the advancement of acute migraine drugs should likely depend on different mechanisms from current 5-HT-related drugs.
机译:简介:20年前舒马曲坦的发展大大增强了5-羟色胺(5-HT)受体的表征及其与急性偏头痛治疗的相关性。最近,没有血管作用的5-HT1F受体激动剂已显示出对偏头痛的治疗功效。涵盖的领域:该评估回顾了针对5-HT受体的急性偏头痛治疗的最新进展。具体来说,作者回顾了5-HT1F受体激动剂以及舒马曲坦和二氢麦角胺(DHE)的新制剂的药代动力学,药效学,临床疗效和安全性。专家意见:Lasmiditan是一种非血管性的5-HT1F受体激动剂,对偏头痛有效,但会引起中枢神经系统相关的不良事件,可能会大大限制其临床应用。透皮舒马曲坦的功效太低,无法普遍用于偏头痛。鼻舒马曲坦粉与口服舒马曲坦相比可能是一个进步,但需要进行对比试验。口服吸入的DHE具有非常快的全身吸收能力,但在偏头痛中起效相对较慢,在2 h后发挥最大作用。相反,口服DHE导致复发率低。这些经过审查的治疗方法均无法满足患者的期望,急性偏头痛药物的进展可能应取决于与目前的5HT相关药物不同的机制。

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