Burnette P K, Perkins J
H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida 33612.
Pharmacotherapy. 1992;12(2):120-31.
Ondansetron hydrochloride dihydrate is a 5-hydroxytryptamine (5-HT3) antagonist that was recently approved by the Food and Drug Administration for the treatment of chemotherapy-induced emesis. The mechanism of action is thought to be due to competitive inhibition of specific serotonin receptors in the central nervous system and gastrointestinal tract. In clinical trials with cisplatin-induced emesis, ondansetron resulted in complete control of vomiting (0-2 episodes) in 55-87% of patients during the first 24 hours of chemotherapy administration. It was significantly more effective than metoclopramide in comparative trials. Ondansetron is also being investigated for the treatment of radiation- and anesthesia-associated nausea and vomiting. Studies in animals demonstrate potential efficacy in the treatment of anxiety, drug withdrawal, and schizophrenia. The drug is generally well tolerated, with no reported extrapyramidal reactions.
盐酸昂丹司琼二水合物是一种5-羟色胺(5-HT3)拮抗剂,最近被美国食品药品监督管理局批准用于治疗化疗引起的呕吐。其作用机制被认为是由于对中枢神经系统和胃肠道中特定血清素受体的竞争性抑制。在顺铂引起的呕吐的临床试验中,昂丹司琼在化疗给药的头24小时内使55%-87%的患者完全控制呕吐(0-2次发作)。在比较试验中,它比甲氧氯普胺显著更有效。昂丹司琼也正在被研究用于治疗放疗和麻醉相关的恶心和呕吐。动物研究表明其在治疗焦虑、药物戒断和精神分裂症方面具有潜在疗效。该药物一般耐受性良好,未报告锥体外系反应。