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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.

DOI:10.1016/j.redar.2012.05.033
PMID:22748853
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。

相似文献

1
[Fospropofol: A new prodrug of propofol].磷丙泊酚:一种新型丙泊酚前体药物
Rev Esp Anestesiol Reanim. 2012 Nov;59(9):497-502. doi: 10.1016/j.redar.2012.05.033. Epub 2012 Jun 30.
2
Fospropofol disodium, a water-soluble prodrug of the intravenous anesthetic propofol (2,6-diisopropylphenol).磷丙泊酚二钠,静脉麻醉药丙泊酚(2,6 - 二异丙基苯酚)的水溶性前体药物。
Expert Opin Investig Drugs. 2009 Oct;18(10):1565-71. doi: 10.1517/13543780903193063.
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Pharmacokinetics and pharmacodynamics of GPI 15715 or fospropofol (Aquavan injection) - a water-soluble propofol prodrug.GPI 15715或磷丙泊酚(水精灵注射液)——一种水溶性丙泊酚前体药物的药代动力学和药效学
Handb Exp Pharmacol. 2008(182):253-66. doi: 10.1007/978-3-540-74806-9_12.
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Fospropofol disodium for sedation.用于镇静的磷丙泊酚二钠
Drugs Today (Barc). 2009 Aug;45(8):567-76. doi: 10.1358/dot.2009.45.8.1396674.
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Fospropofol: a new sedative-hypnotic agent for monitored anesthesia care.福司泊氟酯:一种新型镇静催眠药物,用于监测麻醉护理。
Ann Pharmacother. 2009 Nov;43(11):1802-8. doi: 10.1345/aph.1M290. Epub 2009 Oct 13.
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New drug, fospropofol disodium: a propofol prodrug.新药磷丙泊酚二钠:一种丙泊酚前体药物。
AANA J. 2009 Aug;77(4):301-8.
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Interactive web simulation for propofol and fospropofol, a new propofol prodrug.用于丙泊酚和磷丙泊酚(一种新型丙泊酚前体药物)的交互式网络模拟
Anesth Analg. 2008 Mar;106(3):880-3, table of contents. doi: 10.1213/ane.0b013e3181614fae.
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An improved design of water-soluble propofol prodrugs characterized by rapid onset of action.一种水溶性丙泊酚前药的改良设计,其特点是起效迅速。
Anesth Analg. 2014 Apr;118(4):745-54. doi: 10.1213/ANE.0000000000000124.
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Gastrointestinal delivery of propofol from fospropofol: its bioavailability and activity in rodents and human volunteers.丙泊酚前体药物福米丙泊酚的胃肠道给药:其在啮齿动物和人类志愿者中的生物利用度及活性
J Transl Med. 2015 May 29;13:170. doi: 10.1186/s12967-015-0526-9.
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A randomized, open-label study of the safety and tolerability of fospropofol for patients requiring intubation and mechanical ventilation in the intensive care unit.一项福司泊酚用于 ICU 需插管和机械通气患者的安全性和耐受性的随机、开放标签研究。
Anesth Analg. 2011 Sep;113(3):550-6. doi: 10.1213/ANE.0b013e31821d7faf. Epub 2011 May 19.

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