Welliver Mark, Rugari Susan M
School of Nurse Anesthesia, Harris College of Nursing and Health Sciences, Texas Christian University, Fort Worth, Texas, USA.
AANA J. 2009 Aug;77(4):301-8.
The use of propofol presents chemical and clinical concerns, including pain on injection, allergy risks, possible bacteria growth, and hyperlipidemia. These concerns have encouraged the search for alternative propofol formulations. Elimination of the soybean oil and lecithin carrier agents is difficult because the highly lipophilic diisopropyl phenol molecule does not dissolve in water. Propofol in aqueous solution would be a preferable alternative to lipid-based emulsions. One formulation of propofol is fospropofol disodium (Lusedra, Eisai Corporation of North America, Woodcliff Lake, New Jersey), previously known as Aquavan (MGI Pharma, Bloomington, Minnesota). Fospropofol is an aqueous solution of a propofol prodrug intended for injection. The discovery and development of this drug may address the concerns with the current propofol emulsion formulations while offering altered pharmacokinetics and pharmacodynamics for sedation. The structure, pharmacokinetics, pharmacodynamics, clinical studies, clinical applications, and implications are discussed.
丙泊酚的使用存在化学和临床方面的问题,包括注射疼痛、过敏风险、可能的细菌生长以及高脂血症。这些问题促使人们寻找丙泊酚的替代制剂。由于高度亲脂性的二异丙基苯酚分子不溶于水,因此去除大豆油和卵磷脂载体剂很困难。丙泊酚水溶液将是基于脂质的乳剂的一种更优替代物。丙泊酚的一种制剂是磷丙泊酚二钠(Lusedra,北美卫材公司,新泽西州伍德克利夫湖),以前称为Aquavan(明尼苏达州布卢明顿的MGI制药公司)。磷丙泊酚是一种用于注射的丙泊酚前药的水溶液。这种药物的发现和开发可能解决当前丙泊酚乳剂制剂存在的问题,同时为镇静提供改变的药代动力学和药效学。本文将讨论其结构、药代动力学、药效学、临床研究、临床应用及意义。