丙泊酚

丙泊酚
临床资料
AHFS/Drugs.com	Monograph
怀孕分级	澳: C ; ;
依赖性	生理依赖性：非常高（癫痫发作）; 心理依赖性：无资料
成瘾性	中等
给药途径	静脉注射
ATC码	N01AX10 (WHO) ;
法律规范状态
法律规范	澳：限医生处方（S4）; 加：处方药（℞-only）; 英：处方药（℞-only） (POM); 美：处方药（℞-only）; 处方药（℞-only）;
药物动力学数据
生物利用度	NA
血浆蛋白结合率	95–99%
药物代谢	肝脏 glucuronidation（英语：glucuronidation）
药效起始时间（英语：Onset of action）	15–30 秒
生物半衰期	1.5–31 小时
作用时间	~5–10 分钟
排泄途径	肝脏
识别信息
	IUPAC命名法 2,6-diisopropylphenol; ;
CAS号	2078-54-8
PubChem CID	4943;
IUPHAR/BPS	5464;
DrugBank	DB00818 ;
ChemSpider	4774 ;
UNII	YI7VU623SF;
KEGG	D00549 ;
ChEBI	CHEBI:44915 ;
ChEMBL	ChEMBL526 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID6023523 ;
ECHA InfoCard	100.016.551
化学信息
化学式	C12H18O
摩尔质量	178.28 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES CC(C)c1cccc(c1O)C(C)C;
	InChI InChI=1S/C12H18O/c1-8(2)10-6-5-7-11(9(3)4)12(10)13/h5-9,13H,1-4H3 ; Key:OLBCVFGFOZPWHH-UHFFFAOYSA-N ;

丙泊酚（英语：Propofol），又名异丙酚，商品名得普利麻（Diprivan）及其他。本品为一种短效静脉注射麻醉药，可用于全身麻醉的诱导及维持、成人机械呼吸器（英语：mechanical ventilation）或手术的镇定剂，本品亦可用于治疗其他药物治疗无效的癫痫重积状态。给药后2分钟药效达到最强，且一般可以维持5至10分钟^[4]。

常见的副作用包括心律不整、低血压、注射部位灼热感，以及呼吸中止等等。其他严重的副作用可能包括癫痫发作。不当使用可能会引起感染、成瘾，长期使用则可能导致丙泊酚输注症候群（英语：propofol infusion syndrome）。妊娠期间用药显为安全，但仍有待进一步研究。但不建议用于剖腹生产^[4]。本品并非镇痛药，因此若有镇痛需求，则可以配合吗啡等鸦片类药物使用^[5]。但是否可以常规使用迄今未明^[6]。本品的部分效果可能与其对GABA受体的作用有关^[4]。

丙泊酚最早于1977年发现，美国于1989年核准使用^[4]^[7]。本品列名于世界卫生组织基本药物标准清单之中，为基础公卫体系必备药物之一^[8]。本品专利权已过期，可生产通用名药物^[4]。在发展中国家，每瓶批发价约介于0.61至8.50美金之间^[9]。本品的静脉制剂外观如牛奶一样，常被俗称为“失忆牛奶”、“小牛奶”或“牛奶针”^[10]^[11]。本品亦可作为兽医用药物使用^[12]。

药品介绍

本品无显著蓄积，病人苏醒后头脑清楚，能迅速恢复。用于诱导麻醉和维持麻醉。如果其他药物都没有奏效，它也可用于持续性癫痫状态。它属于静脉给药，最大药效需要大约两分钟后起效，并且通常持续五至十分钟。丙泊酚也常用于兽药。它被50多个国家批准可用。

医疗用途

麻醉

丙泊酚用于麻醉诱导与维持（在某些情况下），因为患者复苏时间快、恢复意识的程度更好从而在很大程度上取代了苯巴比妥类药物硫喷妥钠^[13]。它也可以被施用作为维持麻醉技术的一部分所谓静脉麻醉，使用手动编程输液泵浦或电脑控制输液泵浦，这个过程被称为靶控输注（TCI）。丙泊酚还用于正在接受呼吸机的个体，如患者在重症监护病房。在危重病人身上，丙泊酚在效力和总成本上优于劳拉西泮。

操作医疗程序时对病人的镇静作用

20毫升安瓿1%丙泊酚乳剂，在澳大利亚由山德士销售

丙泊酚也用于手术麻醉(Procedural sedation)，在这些环境中他比咪达唑仑有更快的恢复期。它也可以与类鸦片药物或类苯二氮药物结合使用。由于其快速诱导和快速恢复，丙泊酚也被广泛用于婴儿和儿童接受核磁共振成像检查的镇静作用。它也经常与氯胺酮组合使用，两个一起使用副作用较低。

其他用途

娱乐性使用

已有自我注射丙泊酚进行娱乐性使用的报告^[14]，由于其高强度的效力以及需要安全的医疗监测，使得丙泊酚的娱乐性使用非常危险，自我注射导致的死亡案例被报道^[7]。娱乐性使用短期效果包括轻度欣快感、快速的抗焦虑效果。

参考资料

^ Yang, Man; Zhang, Yinan. Propofol addiction: the mechanism issues we need to know. Anesthesiology and Perioperative Science. 2024-01-08, 2 (1). ISSN 2731-8389. doi:10.1007/s44254-023-00046-y （英语）.
^ Zubair, Salman; Patton, Thomas; Smithson, Kenneth; Sonmezturk, Hasan H.; Arain, Amir; Abou-Khalil, Bassel. Propofol withdrawal seizures: non-epileptic nature of seizures in a patient with recently controlled status epilepticus. Epileptic Disorders: International Epilepsy Journal with Videotape. 2011-03, 13 (1). ISSN 1294-9361. PMID 21393090. doi:10.1684/epd.2011.0404.
^ {{Cite journal |last=Ruffle |first=James K. |title=Molecular neurobiology of addiction: what’s all the (Δ)FosB about? |url=https://www.tandfonline.com/doi/full/10.3109/00952990.2014.933840 |journal=The American Journal of Drug and Alcohol Abuse |language=en |date=2014-11-01 |volume=40 |issue=6 |pages=428–437 |doi=10.3109/00952990.2014.933840 |issn=0095-2990 |pmid=25083822|quote=Propofol is a general anaesthetic, however its abuse for recreational purpose has been documented (120). Using control drugs implicated in both ΔFosB induction and addiction (ethanol and nicotine), similar ΔFosB expression was apparent when propofol was given to rats. Moreover, this cascade was shown to act via the dopamine D1 receptor in the NAc, suggesting that propofol has abuse potential (119)}
^ ^4.0 ^4.1 ^4.2 ^4.3 ^4.4 ^4.5 ^4.6 ^4.7 Propofol. The American Society of Health-System Pharmacists. [2017-01-21]. （原始内容存档于2016-10-09）.
^ Miner, James R.; Burton, John H. Clinical practice advisory: Emergency department procedural sedation with propofol. Annals of Emergency Medicine. 2007-08, 50 (2): 182–187. ISSN 1097-6760. PMID 17321006. doi:10.1016/j.annemergmed.2006.12.017.
^ Wakai, Abel; Blackburn, Carol; McCabe, Aileen; Reece, Emilia; O'Connor, Ger; Glasheen, John; Staunton, Paul; Cronin, John; Sampson, Christopher; McCoy, Siobhan C.; O'Sullivan, Ronan. The use of propofol for procedural sedation in emergency departments. The Cochrane Database of Systematic Reviews. 2015-07-29, 2015 (7): CD007399. ISSN 1469-493X. PMC 6517206  . PMID 26222247. doi:10.1002/14651858.CD007399.pub2.
^ ^7.0 ^7.1 Miller, Ronald D.; Eriksson, Lars I.; Fleisher, Lee A.; Wiener-Kronish, Jeanine P.; Cohen, Neal H.; Young, William L. Miller's Anesthesia E-Book. Elsevier Health Sciences. 2014-10-20. ISBN 978-0-323-28011-2. （原始内容存档于2016-01-29）（英语）.
^ WHO Model List of Essential Medicines (19th List) (PDF). World Health Organization. April 2015 [2016-12-08]. （原始内容存档 (PDF)于2016-12-13）.
^ Propofol. International Drug Price Indicator Guide. [2016-01-23]. （原始内容存档于2021-08-29）.
^ Euliano, T. Y.; Gravenstein, J. S. Essential Anesthesia: From Science to Practice. Cambridge University Press. 2004-12-02: 173. ISBN 978-1-139-45526-8 （英语）.
^ Novick, David M. A Gastroenterologist’s Guide to Gut Health: Everything You Need to Know About Colonoscopy, Digestive Diseases, and Healthy Eating. Rowman & Littlefield. 2017-04-01: 15. ISBN 978-1-4422-7199-9. （原始内容存档于2017-03-29）（英语）.
^ Kesel, M. Lynne. Veterinary Dentistry for the Small Animal Technician. John Wiley & Sons. 2013-05-08: 129. ISBN 978-1-118-69480-0. （原始内容存档于2015-02-01）（英语）.
^ 岚逸筠篁. “牛奶”那些事——浅谈丙泊酚. [2018-10-19]. （原始内容存档于2021-06-05）.
^ Yang, Man; Zhang, Yinan. Propofol addiction: the mechanism issues we need to know. Anesthesiology and Perioperative Science. 2024-01-08, 2 (1). ISSN 2731-8389. doi:10.1007/s44254-023-00046-y （英语）.

外部链接

Diprivan web site run by AstraZeneca
Detailed pharmaceutical information （页面存档备份，存于互联网档案馆）
Propofol. Drug Information Portal. U.S. National Library of Medicine. [2020-11-23]. （原始内容存档于2022-04-15）.
GB patent 1472793,John B Glen & Roger James,“PHARMACEUTICAL COMPOSITIONS”,发表于1977-05-04,指定于Imperial Chemical Industries Ltd （页面存档备份，存于互联网档案馆）

[1] Yang, Man; Zhang, Yinan. Propofol addiction: the mechanism issues we need to know. Anesthesiology and Perioperative Science. 2024-01-08, 2 (1). ISSN 2731-8389. doi:10.1007/s44254-023-00046-y （英语）.

[2] Zubair, Salman; Patton, Thomas; Smithson, Kenneth; Sonmezturk, Hasan H.; Arain, Amir; Abou-Khalil, Bassel. Propofol withdrawal seizures: non-epileptic nature of seizures in a patient with recently controlled status epilepticus. Epileptic Disorders: International Epilepsy Journal with Videotape. 2011-03, 13 (1). ISSN 1294-9361. PMID 21393090. doi:10.1684/epd.2011.0404.

[What_the_ΔFosB?-3] {{Cite journal |last=Ruffle |first=James K. |title=Molecular neurobiology of addiction: what’s all the (Δ)FosB about? |url=https://www.tandfonline.com/doi/full/10.3109/00952990.2014.933840 |journal=The American Journal of Drug and Alcohol Abuse |language=en |date=2014-11-01 |volume=40 |issue=6 |pages=428–437 |doi=10.3109/00952990.2014.933840 |issn=0095-2990 |pmid=25083822|quote=Propofol is a general anaesthetic, however its abuse for recreational purpose has been documented (120). Using control drugs implicated in both ΔFosB induction and addiction (ethanol and nicotine), similar ΔFosB expression was apparent when propofol was given to rats. Moreover, this cascade was shown to act via the dopamine D1 receptor in the NAc, suggesting that propofol has abuse potential (119)}

[AHFS2016-4] 4.0 ^4.1 ^4.2 ^4.3 ^4.4 ^4.5 ^4.6 ^4.7 Propofol. The American Society of Health-System Pharmacists. [2017-01-21]. （原始内容存档于2016-10-09）.

[cpaedpap-5] Miner, James R.; Burton, John H. Clinical practice advisory: Emergency department procedural sedation with propofol. Annals of Emergency Medicine. 2007-08, 50 (2): 182–187. ISSN 1097-6760. PMID 17321006. doi:10.1016/j.annemergmed.2006.12.017.

[:0-6] Wakai, Abel; Blackburn, Carol; McCabe, Aileen; Reece, Emilia; O'Connor, Ger; Glasheen, John; Staunton, Paul; Cronin, John; Sampson, Christopher; McCoy, Siobhan C.; O'Sullivan, Ronan. The use of propofol for procedural sedation in emergency departments. The Cochrane Database of Systematic Reviews. 2015-07-29, 2015 (7): CD007399. ISSN 1469-493X. PMC 6517206  . PMID 26222247. doi:10.1002/14651858.CD007399.pub2.

[:1-7] 7.0 ^7.1 Miller, Ronald D.; Eriksson, Lars I.; Fleisher, Lee A.; Wiener-Kronish, Jeanine P.; Cohen, Neal H.; Young, William L. Miller's Anesthesia E-Book. Elsevier Health Sciences. 2014-10-20. ISBN 978-0-323-28011-2. （原始内容存档于2016-01-29）（英语）.

[WHO19th-8] WHO Model List of Essential Medicines (19th List) (PDF). World Health Organization. April 2015 [2016-12-08]. （原始内容存档 (PDF)于2016-12-13）.

[9] Propofol. International Drug Price Indicator Guide. [2016-01-23]. （原始内容存档于2021-08-29）.

[Euliano-10] Euliano, T. Y.; Gravenstein, J. S. Essential Anesthesia: From Science to Practice. Cambridge University Press. 2004-12-02: 173. ISBN 978-1-139-45526-8 （英语）.

[11] Novick, David M. A Gastroenterologist’s Guide to Gut Health: Everything You Need to Know About Colonoscopy, Digestive Diseases, and Healthy Eating. Rowman & Littlefield. 2017-04-01: 15. ISBN 978-1-4422-7199-9. （原始内容存档于2017-03-29）（英语）.

[12] Kesel, M. Lynne. Veterinary Dentistry for the Small Animal Technician. John Wiley & Sons. 2013-05-08: 129. ISBN 978-1-118-69480-0. （原始内容存档于2015-02-01）（英语）.

[13] 岚逸筠篁. “牛奶”那些事——浅谈丙泊酚. [2018-10-19]. （原始内容存档于2021-06-05）.

[14] Yang, Man; Zhang, Yinan. Propofol addiction: the mechanism issues we need to know. Anesthesiology and Perioperative Science. 2024-01-08, 2 (1). ISSN 2731-8389. doi:10.1007/s44254-023-00046-y （英语）.

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