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化疗引起的恶心和呕吐的药物治疗:关注近期进展

Pharmacological management of chemotherapy-induced nausea and vomiting: focus on recent developments.

作者信息

Navari Rudolph M

机构信息

Department of Medicine, Indiana University School of Medicine, South Bend, USA.

出版信息

Drugs. 2009;69(5):515-33. doi: 10.2165/00003495-200969050-00002.

Abstract

Chemotherapy-induced nausea and vomiting (CINV) is associated with a significant deterioration in quality of life. The emetogenicity of the chemotherapeutic agents, repeated chemotherapy cycles and patient risk factors significantly influence CINV. Serotonin 5-HT(3) receptor antagonists plus dexamethasone have significantly improved the control of acute CINV, but delayed CINV remains a significant clinical problem. Two new agents, palonosetron and aprepitant, have recently been approved for the prevention of both acute and delayed CINV. Palonosetron is a second-generation 5-HT(3) receptor antagonist with a longer half-life and a higher binding affinity than first-generation 5-HT(3) receptor antagonists. Aprepitant is the first agent available in the new drug class of neurokinin-1 (NK-1) receptor antagonists. Casopitant is another NK-1 receptor antagonist, which is under review by the US FDA after recent completion of phase III clinical trials. The introduction of these new agents has generated revised antiemetic guidelines for the prevention of CINV. Future studies may consider the use of palonosetron, aprepitant and casopitant with other antiemetic agents (e.g. olanzapine, gabapentin, cannabinoids) in moderately and highly emetogenic chemotherapy, as well as in the clinical settings of multiple-day chemotherapy and bone marrow transplantation.

摘要

化疗引起的恶心和呕吐(CINV)与生活质量的显著下降相关。化疗药物的致吐性、重复化疗周期以及患者风险因素均会对CINV产生显著影响。5-羟色胺5-HT(3)受体拮抗剂加地塞米松已显著改善了急性CINV的控制,但迟发性CINV仍然是一个重大的临床问题。两种新药,帕洛诺司琼和阿瑞匹坦,最近已被批准用于预防急性和迟发性CINV。帕洛诺司琼是第二代5-HT(3)受体拮抗剂,与第一代5-HT(3)受体拮抗剂相比,半衰期更长,结合亲和力更高。阿瑞匹坦是神经激肽-1(NK-1)受体拮抗剂这一新药类别中的首个药物。卡索匹坦是另一种NK-1受体拮抗剂,在最近完成III期临床试验后正接受美国食品药品监督管理局的审查。这些新药的引入产生了用于预防CINV的修订后止吐指南。未来的研究可能会考虑在中度和高度致吐性化疗中,以及在多日化疗和骨髓移植的临床环境中,将帕洛诺司琼、阿瑞匹坦和卡索匹坦与其他止吐药物(如奥氮平、加巴喷丁、大麻素)联合使用。

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