磷丙泊酚

磷丙泊酚
临床资料
商品名（英语：Drug nomenclature）	Lusedra
AHFS/Drugs.com	Monograph
核准状况	美 FDA: Fospropofol;
怀孕分级	B;
依赖性	未知
给药途径	静脉注射
ATC码	N01 ;
法律规范状态
法律规范	美：附表IV;
药物动力学数据
血浆蛋白结合率	98%
药物代谢	肝葡萄糖醛酸化
生物半衰期	0.81小时
排泄途径	肾
识别信息
	IUPAC命名法 disodium [2,6-di(propan-2-yl)phenoxy]methyl phosphate; ;
CAS号	258516-89-1 ; 258516-87-9（二钠盐）
PubChem CID	3038498;
DrugBank	DB06716 ;
ChemSpider	2302062 ;
UNII	LZ257RZP7K;
KEGG	D04257 ;
ChEMBL	ChEMBL1201766 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID50870295 ;
化学信息
化学式	C13H21O5P
摩尔质量	288.28 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES CC(C)c1cccc(c1OCOP(=O)(O)O)C(C)C;
	InChI InChI=1S/C13H21O5P/c1-9(2)11-6-5-7-12(10(3)4)13(11)17-8-18-19(14,15)16/h5-7,9-10H,8H2,1-4H3,(H2,14,15,16) ; Key:QVNNONOFASOXQV-UHFFFAOYSA-N ;

磷丙泊酚（INN^[3]：Fospropofol），通常以二钠盐（商品名Lusedra^[4]）的形式使用，是一种静脉镇静催眠药。它目前被批准用于接受诊断或治疗程序（如内窥镜检查）的成年患者的镇静。

临床应用

广泛使用的静脉麻醉剂丙泊酚（异丙酚）已开发出多种水溶性衍生物和前药，其中磷丙泊酚已被发现最适合临床开发。^[5]^[6]据称，这种水溶性化合物的优点包括静脉注射部位的疼痛减轻、长期给药引起高脂血症的可能性降低以及感染菌血症的几率降低。^{[来源请求]}通常，磷丙泊酚与芬太尼等阿片类药物联合给药。^{[来源请求]}

临床药理学

作用机制

磷丙泊酚是丙泊酚的前体药物；它被碱性磷酸酶代谢为活性代谢物丙泊酚。

药代动力学

研究人员撤回了磷丙泊酚药代动力学的初步试验结果。截至2011年，尚无新结果。^[7]

管制物质

在美国的《受控物质法》中，磷丙泊酚被归类为附表IV受控物质。^[8]

参考资料

^ ^1.0 ^1.1 Eisai Inc. LUSEDRA (fospropofol disodium) Injection (PDF). Woodcliff Lake, New Jersey: Eisai Inc. October 2009 [2 August 2010]. （原始内容 (PDF)存档于22 November 2010）.
^ Fospropofol disodium. PubChem Compound. Bethesda, Maryland: U.S. National Library of Medicine. [9 February 2017]. （原始内容存档于2023-06-05）.
^ Recommended INNs 2006, pt 56 (PDF). World Health Organization. World Health Organization. [20 April 2016].
^ FDA Approves Fospropofol and Follows ASAs Labeling Recommendation. American Society of Anesthesiologists. 2008-12-15 [2011-03-30]. （原始内容存档于2011-05-26）.
^ Cooke A, Anderson A, Buchanan K, Byford A, Gemmell D, Hamilton N, et al. Water-soluble propofol analogues with intravenous anaesthetic activity. Bioorganic & Medicinal Chemistry Letters. April 2001, 11 (7): 927–30. PMID 11294393. doi:10.1016/S0960-894X(01)00088-9.
^ Bennett DJ, Anderson A, Buchanan K, Byford A, Cooke A, Gemmell DK, et al. Novel water soluble 2,6-dimethoxyphenyl ester derivatives with intravenous anaesthetic activity. Bioorganic & Medicinal Chemistry Letters. June 2003, 13 (12): 1971–5. PMID 12781176. doi:10.1016/S0960-894X(03)00346-9.
^ Mahajan B, Kaushal S, Mahajan R. Fospropofol: pharmacokinetics?. Journal of Anaesthesiology Clinical Pharmacology. January 2012, 28 (1): 134–5. PMC 3275955  . PMID 22345970. doi:10.4103/0970-9185.92472.
^ "Schedule of Controlled Substances; Placement of Fospropofol into Schedule IV^{[永久失效链接]}," 74 Federal Register 192 (October 6, 2009), pp. 51234–51236.

[Eisai2009-1] 1.0 ^1.1 Eisai Inc. LUSEDRA (fospropofol disodium) Injection (PDF). Woodcliff Lake, New Jersey: Eisai Inc. October 2009 [2 August 2010]. （原始内容 (PDF)存档于22 November 2010）.

[PubChem-2] Fospropofol disodium. PubChem Compound. Bethesda, Maryland: U.S. National Library of Medicine. [9 February 2017]. （原始内容存档于2023-06-05）.

[3] Recommended INNs 2006, pt 56 (PDF). World Health Organization. World Health Organization. [20 April 2016].

[4] FDA Approves Fospropofol and Follows ASAs Labeling Recommendation. American Society of Anesthesiologists. 2008-12-15 [2011-03-30]. （原始内容存档于2011-05-26）.

[5] Cooke A, Anderson A, Buchanan K, Byford A, Gemmell D, Hamilton N, et al. Water-soluble propofol analogues with intravenous anaesthetic activity. Bioorganic & Medicinal Chemistry Letters. April 2001, 11 (7): 927–30. PMID 11294393. doi:10.1016/S0960-894X(01)00088-9.

[6] Bennett DJ, Anderson A, Buchanan K, Byford A, Cooke A, Gemmell DK, et al. Novel water soluble 2,6-dimethoxyphenyl ester derivatives with intravenous anaesthetic activity. Bioorganic & Medicinal Chemistry Letters. June 2003, 13 (12): 1971–5. PMID 12781176. doi:10.1016/S0960-894X(03)00346-9.

[7] Mahajan B, Kaushal S, Mahajan R. Fospropofol: pharmacokinetics?. Journal of Anaesthesiology Clinical Pharmacology. January 2012, 28 (1): 134–5. PMC 3275955  . PMID 22345970. doi:10.4103/0970-9185.92472.

[8] "Schedule of Controlled Substances; Placement of Fospropofol into Schedule IV^{[永久失效链接]}," 74 Federal Register 192 (October 6, 2009), pp. 51234–51236.

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