Saxena P R, Den Boer M O
Department of Pharmacology, Faculty of Medicine, Erasmus University, Rotterdam, The Netherlands.
J Neurol. 1991;238 Suppl 1:S28-35. doi: 10.1007/BF01642903.
The drugs used in migraine therapy can be divided into two groups: agents that abort an established migraine attack and agents used prophylactically to reduce the number of migraine attacks. Both groups have drugs that are specific for migrainous headaches and that are non-specific, and are used to treat the accompanying headache (analgesics), vomiting (anti-emetics), anxiety (sedatives and anxiolytics), or depression (antidepressants). The main drugs with specific action on migraine include ergot alkaloids (ergotamine, dihydroergotamine), agonists (sumatriptan) or partial agonists (methysergide) at a specific subtype of 5-HT1-like receptors, beta-adrenoceptor antagonists (propranolol, metoprolol), calcium antagonists (flunarizine) and anti-inflammatory agents (indomethacin). The pharmacological basis of therapeutic action of several of these drugs is not well understood. In the case of the ergot alkaloids and 5-HT1-like receptor agonists, however, it is likely that the antimigraine effect is related to the potent and rather selective constriction of the large arteries and arteriovenous anastomoses in the scalp and dural regions. In addition, these drugs inhibit plasma extravasation into the dura in response to trigeminal ganglion stimulation, but it is possible that this effect is related to the selective vasoconstriction in the extracerebral vascular bed. The selectivity of the pharmacological effects of these antimigraine drugs (constriction of the extracerebral arteries and arteriovenous anastomoses, poor penetration into the central nervous system and the absence of an antinociceptive effect even after intrathecal administration) strongly suggests that excessive dilatation in the extracerebral cranial vasculature, probably initiated by a neuronal event, is an integral part of the pathophysiology of migraine.
用于终止已发作偏头痛的药物和用于预防性减少偏头痛发作次数的药物。这两类药物中都有对偏头痛性头痛具有特异性的药物以及非特异性药物，后者用于治疗伴随的头痛（镇痛药）、呕吐（止吐药）、焦虑（镇静剂和抗焦虑药）或抑郁（抗抑郁药）。对偏头痛具有特异性作用的主要药物包括麦角生物碱（麦角胺、二氢麦角胺）、5-HT1样受体特定亚型的激动剂（舒马曲坦）或部分激动剂（美西麦角）、β-肾上腺素能受体拮抗剂（普萘洛尔、美托洛尔）、钙拮抗剂（氟桂利嗪）和抗炎药（吲哚美辛）。其中几种药物治疗作用的药理学基础尚未完全明确。然而，就麦角生物碱和5-HT1样受体激动剂而言，其抗偏头痛作用可能与头皮和硬脑膜区域大动脉及动静脉吻合支的强效且相当选择性的收缩有关。此外，这些药物可抑制三叉神经节刺激引起的血浆向硬脑膜的外渗，但这种作用可能与脑外血管床的选择性血管收缩有关。这些抗偏头痛药物药理作用的选择性（脑外动脉和动静脉吻合支的收缩、难以穿透中枢神经系统以及即使鞘内给药也无抗伤害感受作用）强烈提示，可能由神经元事件引发的脑外颅血管过度扩张是偏头痛病理生理学的一个重要组成部分。
