Seynaeve C, Verweij J, de Mulder P H
Department of Medical Oncology, Rotterdam Cancer Institute/Dr Daniel den Hoed Kliniek, The Netherlands.
Anticancer Drugs. 1991 Aug;2(4):343-55. doi: 10.1097/00001813-199108000-00003.
In recent years a new class of agents, the serotonin type 3 receptor antagonists, has been identified. This article reviews the preclinical, pharmacological and clinical data of ondansetron, granisetron and tropisetron, the first representatives of this group. Preclinical work showed that the drugs interfere with a variety of physiological processes, and hold promise for clinical utility in a wide range of areas. To date, these agents have proven, both in early clinical and comparative studies, to be potent antiemetic agents in patients receiving cisplatin and non-cisplatin chemotherapy as well as radiotherapy. In comparative studies the antiemetic efficacy mostly has been superior to conventional antiemetic drugs with regard to the acute chemotherapy-related symptoms; whereas their role in delayed emesis needs further investigation. This also applies for their role as an antiemetic in other types of nausea and vomiting (post-operative). Toxic effects have been modest, no extrapyramidal reactions have been reported. Potential clinical use in psychiatric disorders has been suggested, and the results of clinical trials are awaited.
近年来，已鉴定出一类新型药物——5-羟色胺3型受体拮抗剂。本文回顾了该类药物的首批代表药物昂丹司琼、格拉司琼和托烷司琼的临床前、药理学及临床数据。临床前研究表明，这些药物可干扰多种生理过程，并有望在广泛领域发挥临床效用。迄今为止，在早期临床研究和对照研究中均已证实，这些药物对于接受顺铂和非顺铂化疗以及放疗的患者而言，是有效的止吐药。在对照研究中，就急性化疗相关症状而言，其止吐疗效大多优于传统止吐药物；而它们在迟发性呕吐中的作用尚需进一步研究。这同样适用于它们在其他类型恶心和呕吐（术后）中作为止吐药的作用。毒性作用较小，未报告有锥体外系反应。已有人提出它们在精神疾病中的潜在临床用途，有待临床试验结果。
