Whealy Mark, Becker Werner J
Department of Neurology, Mayo Clinic, Rochester, MN, United States.
Department of Clinical Neurosciences, Cumming School of Medicine, University of Calgary, and Hotchkiss Brain Institute, Calgary, AB, Canada.
Handb Clin Neurol. 2024;199:17-42. doi: 10.1016/B978-0-12-823357-3.00008-2.
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-HT and 5-HT 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.
曲坦类药物的出现彻底改变了急性偏头痛的治疗方法。较早的偏头痛特异性药物麦角生物碱（麦角胺和双氢麦角胺）也通过作用于5-HT和5-HT受体来缓解偏头痛发作，但曲坦类药物对这些受体具有更高的特异性。与麦角生物碱不同，曲坦类药物不会激活许多其他受体类型，因此耐受性更好。副作用的减少极大地提高了它们的临床实用性，因为这使得更大比例的患者能够服用完整的治疗剂量。结果，如今麦角胺的临床应用极少，尽管双氢麦角胺仍具有重要的临床作用。有大量证据表明，如今可用的七种曲坦类药物，即舒马曲坦、佐米曲坦、利扎曲坦、依立曲坦、那拉曲坦、阿莫曲坦和夫罗曲坦，在偏头痛的急性治疗中是有效的。可用剂型包括口服片剂、口腔崩解片、皮下注射剂、鼻喷雾剂，在一些国家还有直肠栓剂。为了获得最佳疗效，对于特定患者，在选择曲坦类药物和剂型方面都需要进行个体化治疗。本章讨论麦角生物碱和曲坦类药物，包括作用机制、疗效证据、临床应用和不良反应。
