Aapro M S
Clinique de Genolier and Hôpital Cantonal Universitaire, Geneva, Switzerland.
Ann Oncol. 1993;4 Suppl 3:9-14. doi: 10.1093/annonc/4.suppl_3.s9.
Development of the serotonin type 3 (5-HT3) receptor antagonists has facilitated a new understanding of the physiology of emesis. Three new agents, ondansetron, granisetron and tropisetron, are currently available in several countries and this review will focus on the characteristics of ondansetron and granisetron, so that a perspective of the data for tropisetron can be presented by other authors. Preclinical data indicate some possible differences among these new compounds. They differ in pharmacokinetic terms. Efficacy and a good safety profile for acute emesis control have been demonstrated for both agents, although there may be some debate as to the best schedule of ondansetron. Delayed emesis does not seem to be adequately controlled by these drugs, and they may also lose some efficacy during multiple-day chemotherapy or after several cycles of chemotherapy. While the addition of corticosteroids seems to increase the response rate to ondansetron, no such data are yet available for granisetron. Finally, considerations pertinent to the cost of these new agents are discussed.
5-羟色胺3（5-HT3）受体拮抗剂的开发促进了对呕吐生理学的新认识。目前有三种新药，昂丹司琼、格拉司琼和托烷司琼在多个国家上市，本综述将重点关注昂丹司琼和格拉司琼的特性，以便其他作者能够介绍托烷司琼的数据情况。临床前数据表明这些新化合物之间可能存在一些差异。它们在药代动力学方面有所不同。两种药物在控制急性呕吐方面均已证明具有疗效且安全性良好，尽管对于昂丹司琼的最佳给药方案可能存在一些争议。这些药物似乎无法充分控制延迟性呕吐，而且在多日化疗期间或几个化疗周期后它们可能也会失去一些疗效。虽然添加皮质类固醇似乎可提高对昂丹司琼的反应率，但目前尚无格拉司琼的此类数据。最后，讨论了与这些新药成本相关的问题。
