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磷丙泊酚:一种新型丙泊酚前体药物

[Fospropofol: A new prodrug of propofol].

作者信息

Telletxea S, Lauzirika Z, Etxebarria A, Ortega L F

机构信息

Servicio de Anestesiología, Reanimación y Terapia del Dolor, Hospital de Galdakao, Bizkaia, España.

出版信息

Rev Esp Anestesiol Reanim. 2012 Nov;59(9):497-502. doi: 10.1016/j.redar.2012.05.033. Epub 2012 Jun 30.

Abstract

The development of new propofol formulations has advanced rapidly in the last ten years with the achievement of the marketing a new prodrug of propofol: fospropofol, pharmacologically different from the original compound. It is a water soluble compound that requires metabolism of the prodrug to propofol, which leads to a time delay between its administration and the appearance of its pharmacological effect. Its pharmacokinetic and pharmacodynamic characteristics are different to the original formula. Due to its formulation it does not cause pain on intravenous injection, does not lead to hyperlipidaemia or excess bacterial growth. Although it is currently unavailable in Spain, it has been approved by the FDA (American Food and Drug Administration) for sedation in controlled care in diagnostic and therapeutic procedures in adults. It must only be administered by personnel qualified to administer anaesthesia, and the patients must be monitored throughout the whole procedure.

摘要

在过去十年中,新型丙泊酚制剂的研发进展迅速,一种新型丙泊酚前体药物——磷丙泊酚已上市,其药理特性与原化合物不同。它是一种水溶性化合物,需要将前体药物代谢为丙泊酚,这导致给药与药理作用出现之间存在时间延迟。其药代动力学和药效学特性与原配方不同。由于其制剂特点,静脉注射时不会引起疼痛,不会导致高脂血症或细菌过度生长。尽管目前在西班牙无法获得,但它已获得美国食品药品监督管理局(FDA)批准,用于成人诊断和治疗程序的监护镇静。它必须仅由有资格实施麻醉的人员给药,并且在整个过程中必须对患者进行监测。

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