Schwarzberg M N
Headache. 1994 Jul-Aug;34(7):439-41. doi: 10.1111/j.1526-4610.1994.hed3407439.x.
The 5-HT3 antagonism property of metoclopramide, acting on receptors presumably located in the trigeminovascular system, is the theoretical basis of its remarkable success, as a single intravenous agent, in the treatment of migraine attacks. The specific anti-migraine activity of oral metoclopramide is, most probably, applicable only when its plasma level is equivalent to 10 mg injected intravenously. The clinical effective dose of ergotamine, beginning from the minimal dose of 1 mg, correlates well with its affinity for 5-HT1B and 5-HT1D receptors, and the rank order of clinical potency of ergotamine is superior to sumatriptan. The presumed synergic power of drugs that interact with both 5-HT1 and 5-HT3 receptors is examined, in order to formulate a highly potent, low headache recurrence, oral combination.
甲氧氯普胺的5-羟色胺3（5-HT3）拮抗特性作用于可能位于三叉神经血管系统的受体，这是其作为单一静脉用药在治疗偏头痛发作方面取得显著成功的理论基础。口服甲氧氯普胺的特异性抗偏头痛活性，很可能仅在其血浆水平等同于静脉注射10毫克时才适用。麦角胺的临床有效剂量从最小剂量1毫克开始，与其对5-羟色胺1B（5-HT1B）和5-羟色胺1D（5-HT1D）受体的亲和力密切相关，且麦角胺的临床效力等级顺序优于舒马曲坦。为了配制一种高效、低头痛复发率的口服组合药物，对与5-HT1和5-HT3受体都相互作用的药物的假定协同作用进行了研究。
