Tsukagoshi S
Cancer Chemotherapy Center, Japanese Fundation for Cancer Research.
Gan To Kagaku Ryoho. 1999 Jun;26(7):1001-8.
5-HT3 receptor antagonists have been established in a number of clinical trials as effective agents in the management of nausea and vomiting induced by cancer chemotherapy including cisplatin. Azasetron (Serotone) is a potent and selective 5-HT3 receptor antagonist, and classified as benzamide derivative. It has a different chemical structure from indole-type 5-HT3 receptor antagonists such as granisetron, ondansetron, ramosetron and tropisetron. The major difference is found in the pharmacokinetic profiles. Approximately 60-70% of azasetron administered i.v. and orally is excreted in urine as the unmetabolized form. Also, orally-administered azasetron has shown to be absorbed and/or secreted by the saturable transport mechanism in the small intestine, resulting in good bioavailability as approximately 90%. In this report, the relationship between the structure of 5-HT3 receptor antagonists (especially azasetron) and their pharmacokinetics were described.
5-HT3受体拮抗剂已在多项临床试验中被确立为治疗包括顺铂在内的癌症化疗引起的恶心和呕吐的有效药物。阿扎司琼（Serotone）是一种强效且选择性的5-HT3受体拮抗剂，属于苯甲酰胺衍生物。它与吲哚型5-HT3受体拮抗剂如格拉司琼、昂丹司琼、雷莫司琼和托烷司琼具有不同的化学结构。主要差异在于药代动力学特征。静脉注射和口服给药的阿扎司琼约60%-70%以未代谢形式经尿液排泄。此外，口服阿扎司琼已显示可通过小肠中的饱和转运机制被吸收和/或分泌，导致良好的生物利用度，约为90%。在本报告中，描述了5-HT3受体拮抗剂（尤其是阿扎司琼）的结构与其药代动力学之间的关系。
