关键词: Abortive Acute Dihydroergotamine Ergot Ergotamine Migraine Treatment Triptan

Mesh : Humans Dihydroergotamine / therapeutic use Ergotamine / therapeutic use Migraine Disorders / drug therapy Serotonin / therapeutic use Tryptamines / therapeutic use Serotonin 5-HT1 Receptor Agonists / therapeutic use

来  源:   DOI:10.1016/B978-0-12-823357-3.00008-2

Abstract:
The advent of the triptans revolutionized acute migraine treatment. The older migraine-specific drugs, the ergot alkaloids (ergotamine and dihydroergotamine), also relieve migraine attacks through agonism at the 5-HT1B and 5-HT1D receptors, but the triptans have much greater specificity for these receptors. Unlike the ergot alkaloids, the triptans do not activate many other receptor types, and therefore are much better tolerated. This reduction in side effects greatly enhanced their clinical utility as it allowed a far greater proportion of patients to take a full therapeutic dose. As a result, the clinical use of ergotamine is minimal today, although dihydroergotamine still has a significant clinical role. There is extensive evidence that the seven triptans available today, sumatriptan, zolmitriptan, rizatriptan, eletriptan, naratriptan, almotriptan, and frovatriptan, are effective in the acute treatment of migraine. Available formulations include oral tablets, orally dissolving tablets, subcutaneous injections, nasal sprays, and in some countries, rectal suppositories. For optimal benefit, therapy needs to be individualized for a given patient both regarding the triptan chosen and the formulation. This chapter discusses the ergot alkaloids and the triptans, including mechanism of action, evidence for efficacy, clinical use, and adverse effects.
摘要:
曲坦类药物的出现彻底改变了急性偏头痛的治疗方法。较老的偏头痛特异性药物,麦角生物碱(麦角胺和双氢麦角胺),还可以通过5-HT1B和5-HT1D受体的激动来缓解偏头痛的发作,但是曲坦类药物对这些受体有更大的特异性。不像麦角生物碱,曲坦类药物不会激活许多其他受体类型,因此有更好的耐受性。这种副作用的减少极大地增强了它们的临床效用,因为它允许更大比例的患者服用全治疗剂量。因此,今天麦角胺的临床使用很少,尽管二氢麦角胺仍具有重要的临床作用。有大量证据表明,今天可用的七种triptans,舒马曲坦,佐米曲坦,利扎曲普坦,依来曲坦,那拉曲坦,阿莫曲坦,还有Frovatriptan,对偏头痛的急性治疗有效。可用的配方包括口服片剂,口服溶解片剂,皮下注射,鼻腔喷雾剂,在一些国家,直肠栓剂.为了获得最佳效益,对于给定的患者,治疗需要在选择的曲坦和制剂方面进行个性化。本章讨论麦角生物碱和曲坦,包括作用机制,有效性的证据,临床使用,和不利影响。
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