Albibi R, McCallum R W
Ann Intern Med. 1983 Jan;98(1):86-95. doi: 10.7326/0003-4819-98-1-86.
Metoclopramide antagonizes the effect of dopamine in the central nervous system and other organ systems. Metoclopramide's effect on the medullary chemoreceptor trigger zone makes it useful as a routine anti-emetic and in preventing vomiting induced by antineoplastic drugs, particularly cisplatin. Metoclopramide's gastrointestinal smooth muscle stimulatory effects are related to its ability to antagonize the inhibitory neurotransmitter, dopamine; to augment acetylcholine release and sensitize the muscarinic receptors of the gastrointestinal smooth muscle; and to coordinate gastric-pyloric-small intestinal motor function. The indications for which metoclopramide is approved in the United States are reviewed. Adverse effects, which may occur in up to 20% of patients, include drowsiness, lassitude, and akathisia; all are usually mild, transient, and reversible. Tremor, dystonic reactions, and extrapyramidal effects are infrequent; breast enlargement, galactorrhea, and menstrual irregularities are related to prolactin release.
甲氧氯普胺可拮抗多巴胺在中枢神经系统和其他器官系统中的作用。甲氧氯普胺对延髓化学感受器触发区的作用使其成为常用的止吐药,并可用于预防抗肿瘤药物(尤其是顺铂)引起的呕吐。甲氧氯普胺对胃肠道平滑肌的刺激作用与其拮抗抑制性神经递质多巴胺的能力有关;增加乙酰胆碱释放并使胃肠道平滑肌的毒蕈碱受体敏感;并协调胃 - 幽门 - 小肠的运动功能。本文综述了美国批准使用甲氧氯普胺的适应症。高达20%的患者可能出现不良反应,包括嗜睡、倦怠和静坐不能;所有这些通常都是轻微、短暂且可逆的。震颤、肌张力障碍反应和锥体外系反应很少见;乳房增大、溢乳和月经不调与催乳素释放有关。