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二氢麦角胺、麦角胺、麦角乙脲和舒马曲坦——与偏头痛治疗相关的基础科学。

Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment.

机构信息

Gothenburg Migraine Clinic AB, Gothenburg, Sweden.

出版信息

Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22.

Abstract

The 5-hydroxytryptamine (5-HT) receptor family mediates the effects of several drugs highly effective in migraine primarily by activating 5-HT(1B) , 5-HT(1D) , and 5-HT(1F) receptors. Ergotamine, dihydroergotamine, and methysergide, as well as the "triptan" sumatriptan, are all agonists for these receptors. The receptor profile and degree of selectivity of these four drugs differ, which is reflected by their side effects that limit their use in the acute and prophylactic treatment of migraine. The acute antimigraine efficacy of these remedies is very much dependent on the formulation used where, in general, parenteral formulations are more effective in reliving the symptoms of a migraine attack.

摘要

5-羟色胺(5-HT)受体家族介导了几种在偏头痛中非常有效的药物的作用,主要通过激活 5-HT(1B)、5-HT(1D)和 5-HT(1F)受体。麦角胺、二氢麦角胺和麦角乙脲以及“曲坦”类药物舒马曲坦都是这些受体的激动剂。这四种药物的受体谱和选择性程度不同,这反映在它们的副作用上,这些副作用限制了它们在偏头痛的急性和预防性治疗中的应用。这些药物的急性抗偏头痛疗效在很大程度上取决于所使用的制剂,一般来说,肠外制剂在缓解偏头痛发作的症状方面更有效。

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