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Ondansetron是5-羟色胺(5-HT)的拮抗剂。已在美国上市,静脉给药以防止癌症化疗引起的恶心和呕吐,许多国家则使用口服制剂。药理学Ondansetron在上消化道传入迷走神经末端5-HT_3受体上和中枢神经系统化学受体触发区,对5-HT的去极化有拮抗作用。与甲氧氯普胺、丙氯丙嗪不同,Ondansetron不捕抗多巴胺能的活性,因此不会引起锥体外系的不良反应。该药主要在肝内代谢,其代谢产物经尿排除,半衰期3.5小时。老年人及严重肝功能不全者,此药半衰期将会延长。临床试验在接受顺铂及其他抗癌药物治疗的患者中,Ondansetron有明显止吐作用。有一报道在35例患者接受顺铂治疗的4～5天中反复给予Ondansetron。
Ondansetron is an antagonist of serotonin (5-HT). It has been marketed in the United States and administered intravenously to prevent nausea and vomiting from cancer chemotherapy. Many countries use oral preparations. The pharmacological Ondansetron enters the vagal nerve terminal 5-HT3 receptor in the upper gastrointestinal tract and triggers the chemical receptors in the central nervous system, which may antagonize the depolarization of 5-HT. Unlike metoclopramide and prochlorperazine, Ondansetron does not capture antidopaminergic activity and therefore does not cause extrapyramidal adverse reactions. The drug is mainly metabolized in the liver. Its metabolites are eliminated in urine and have a half-life of 3.5 hours. Elderly people and severe liver dysfunction, the drug half-life will be extended. Clinical trials Ondansetron has significant antiemetic effects in patients receiving cisplatin and other anticancer drugs. One report repeatedly gave Ondansetron in 4 to 5 days of 35 patients receiving cisplatin treatment.