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新型依托咪酯衍生物。

Novel etomidate derivatives.

机构信息

Playmouth University, Peninsula School of Medicine and Dentistry, Tamar Science Park, UK.

出版信息

Curr Pharm Des. 2012;18(38):6253-6. doi: 10.2174/138161212803832362.

Abstract

Etomidate is a well established intravenous anaesthetic agent which has been widely used. Recognised limitations of the agent include adrenocortical suppression, myoclonus and post-operative nausea and vomiting, PONV. MOC-etomidate, carboetomidate and MOC-carboetomidate are novel etomidate derivatives. Their preclinical data and their potential for human administration are critically reviewed. 'Soft' pharmacology (rapid ester hydrolysis) limits the duration of action of MOC-etomidate and MOC-carboetomidate giving them rapid offset after administration is discontinued. Adrenocortical depression is minimised either by ester hydrolysis or by structural change to the etomidate molecule. Potential limitations include the yet to be determined incidence of myoclonus and PONV if these new agents are administered to humans.

摘要

依托咪酯是一种已被广泛应用的成熟的静脉麻醉剂。其公认的局限性包括肾上腺皮质抑制、肌阵挛和术后恶心和呕吐(PONV)。MOC-依托咪酯、卡泊依托咪酯和 MOC-卡泊依托咪酯是新型依托咪酯衍生物。对其临床前数据及其在人类中的应用潜力进行了批判性评价。“软”药理学(快速酯水解)限制了 MOC-依托咪酯和 MOC-卡泊依托咪酯的作用持续时间,使其在停药后迅速消退。通过酯水解或依托咪酯分子结构的改变,最大限度地减少肾上腺皮质抑制。潜在的局限性包括这些新药物如果被用于人类,尚未确定的肌阵挛和 PONV 的发生率。

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