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5-羟色胺3型受体拮抗剂用于术后恶心和呕吐的药理学、药物遗传学及临床疗效

Pharmacology, pharmacogenetics, and clinical efficacy of 5-hydroxytryptamine type 3 receptor antagonists for postoperative nausea and vomiting.

作者信息

Ho Kok-Yuen, Gan Tong J

机构信息

Department of Anesthesiology, Duke University Medical Center, Durham, North Carolina 27710, USA.

出版信息

Curr Opin Anaesthesiol. 2006 Dec;19(6):606-11. doi: 10.1097/01.aco.0000247340.61815.38.

DOI:10.1097/01.aco.0000247340.61815.38
PMID:17093363
Abstract

PURPOSE OF REVIEW

The use of selective 5-hydroxytryptamine type 3 receptor antagonists has improved the management of postoperative nausea and vomiting, but has not completely eliminated it. In this article, we discuss the pharmacology of 5-hydroxytryptamine type 3 receptor antagonists and the impact of pharmacogenetics on postoperative nausea and vomiting.

RECENT FINDINGS

Dolasetron, granisetron, ondansetron, palonosetron, and tropisetron have similar mechanisms of action but different pharmacokinetic and pharmacodynamic properties. Genetic polymorphism in the cytochrome P450 mono-oxygenase system, drug efflux transporter adenosine triphosphate-binding cassette subfamily B member 1 and 5-hydroxytryptamine type 3 receptor subunits also contribute to the interindividual variation in response to different 5-hydroxytryptamine type 3 receptor antagonists. These differences account for differences in the duration of action and clinical efficacy of these agents.

SUMMARY

Pharmacogenetics testing in patients may help differentiate responders to 5-hydroxytryptamine type 3 receptor antagonists from non-responders and allow the anesthesiologist to individualize antiemetic therapy. The cost-effectiveness of such screening in postoperative nausea and vomiting management has, however, not been evaluated. Given the multifactorial nature of postoperative nausea and vomiting, a multimodal approach to reduce or eliminate risk factors will be most successful in its management.

摘要

综述目的

5-羟色胺3型受体拮抗剂的应用改善了术后恶心呕吐的治疗,但尚未完全消除该症状。在本文中,我们讨论了5-羟色胺3型受体拮抗剂的药理学以及药物遗传学对术后恶心呕吐的影响。

最新发现

多潘立酮、格拉司琼、昂丹司琼、帕洛诺司琼和托烷司琼具有相似的作用机制,但药代动力学和药效学特性不同。细胞色素P450单加氧酶系统、药物外排转运体三磷酸腺苷结合盒亚家族B成员1和5-羟色胺3型受体亚基的基因多态性也导致了个体对不同5-羟色胺3型受体拮抗剂反应的差异。这些差异解释了这些药物作用持续时间和临床疗效的不同。

总结

对患者进行药物遗传学检测可能有助于区分5-羟色胺3型受体拮抗剂的反应者和无反应者,并使麻醉医生能够个体化抗呕吐治疗。然而,这种筛查在术后恶心呕吐管理中的成本效益尚未得到评估。鉴于术后恶心呕吐的多因素性质,采用多模式方法减少或消除危险因素将最成功地管理该症状。

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