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氯丙嗪

氯丙嗪
Skeletal formula of chlorpromazine
Ball-and-stick model of the chlorpromazine molecule
临床资料
商品名英语Drug nomenclatureLargactil, Thorazine, others
AHFS/Drugs.comMonograph
MedlinePlusa682040
核准状况
怀孕分级
  • : C
给药途径口服(药丸或糖浆)、肛门塞剂肌肉注射静脉注射
ATC码
法律规范状态
法律规范
药物动力学数据
生物利用度10–80%(口服,视体质而定)[1]
血浆蛋白结合率90–99%[1]
药物代谢肝脏,大多经CYP2D6[1]
生物半衰期30 小时[2]
排泄途径尿液(24小时内排除43–65%)[1]
识别信息
  • 3-(2-chloro-10H-phenothiazin-10-yl)-N,N-dimethyl-propan-1-amine
CAS号50-53-3(自由基团)  checkY
69-09-0(盐酸盐)
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.000.042 编辑维基数据链接
化学信息
化学式C17H19ClN2S
摩尔质量318.86 g/mol(自由基团)
355.33 g/mol(盐酸盐)
3D模型(JSmol英语JSmol
  • CN(C)CCCN1c2ccccc2Sc3c1cc(cc3)Cl
  • InChI=1S/C17H19ClN2S/c1-19(2)10-5-11-20-14-6-3-4-7-16(14)21-17-9-8-13(18)12-15(17)20/h3-4,6-9,12H,5,10-11H2,1-2H3 checkY
  • Key:ZPEIMTDSQAKGNT-UHFFFAOYSA-N checkY

氯丙嗪(Chlorpromazine,简称CPZ),常见商标名 ThorazineLargactil,是一种精神科药物[2]。本品一般用于治疗精神分裂症思觉失调[2]。其他用途还可用做作治疗躁郁症过动症恶心呕吐、术前焦虑,或是其他方法无法控制的打嗝症状等等[2]。本品可以口服、肌肉注射静脉注射[2]

常见副作用包含锥体外症候群嗜睡、口干、姿位性低血压,以及体重增加等等[2]。严重副作用可能导致迟发性不自主运动英语tardive dyskinesia等永久运动功能障碍、抗精神药物恶性症候群英语neuroleptic malignant syndrome、以及白细胞减少症[2]。因失智症导致精神错乱的老年人用药可能会增加死亡风险[2]妊娠期间用药的安全性迄今不明[2]。本品属于典型抗忧郁药物英语typical antipsychotic[2]。其作用机制尚未明朗,但可能与其具多巴胺受体拮抗剂英语dopamine antagonist的活性有关[2]。本品亦具有抗血清素英语antiserotonergic以及抗组织胺的活性[2]

本品最早于1950年发现,为第一种精神疾患药物[3][4]。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[5]。氯丙嗪的发现为精神医疗的重大里程碑英语history of psychiatry[6][7]。本品属于通用名药物[2],其于发展中国家的每日剂量批发价约介于 0.02 至 0.12 美金之间[8]。在美国同样剂量则约需 2 美金[2]

药理学

现在氯丙嗪被归入第一代抗精神病药,它们的药理机制是阻断脑内多巴胺受体,从而发挥抗精神病作用。

不良反应

该类药物一般都伴有锥体外系副作用。针剂的体位性低血压副作用较明显。长期服用后戒断会出现肌肉抽搐

剂型及用量

有片剂和针剂,25mg/片,50mg/针。

用于治疗精神病时起始剂量较低,根据病人情况逐渐加量至治疗剂量,治疗剂量一般在300mg至600mg之间。该药有较强的镇静作用,故也常用于镇静。针剂通常用于不合作病人,另外针剂通常与盐酸异丙嗪(也叫非那根)合用,组成冬非合剂。

注释

  1. ^ 1.0 1.1 1.2 1.3 PRODUCT INFORMATION LARGACTIL (PDF). TGA eBusiness Services. Sanofi Aventis Pty Ltd. 28 August 2012 [8 December 2013]. (原始内容存档于30 March 2017). 
  2. ^ 2.00 2.01 2.02 2.03 2.04 2.05 2.06 2.07 2.08 2.09 2.10 2.11 2.12 2.13 Chlorpromazine Hydrochloride. The American Society of Health-System Pharmacists. [Dec 1, 2015]. (原始内容存档于8 December 2015). 
  3. ^ López-Muñoz, Francisco; Alamo, Cecilio; Cuenca, Eduardo; Shen, Winston W.; Clervoy, Patrick; Rubio, Gabriel. History of the discovery and clinical introduction of chlorpromazine. Annals of Clinical Psychiatry. 2005, 17 (3): 113–35. PMID 16433053. doi:10.1080/10401230591002002. 
  4. ^ Ban, TA. Fifty years chlorpromazine: a historical perspective.. Neuropsychiatric disease and treatment. August 2007, 3 (4): 495–500. PMC 2655089可免费查阅. PMID 19300578. 
  5. ^ WHO Model List of Essential Medicines (19th List) (PDF). World Health Organization. April 2015 [8 December 2016]. (原始内容存档 (PDF)于13 December 2016). 
  6. ^ López-Muñoz, F; Alamo, C; Cuenca, E; Shen, WW; Clervoy, P; Rubio, G. History of the discovery and clinical introduction of chlorpromazine.. Annals of Clinical Psychiatry. 2005, 17 (3): 113–35. PMID 16433053. doi:10.1080/10401230591002002. 
  7. ^ Shorter, Edward. A historical dictionary of psychiatry. New York: Oxford University Press. 2005: 6. ISBN 9780198039235. (原始内容存档于14 February 2017). 
  8. ^ Chlorpromazine HCL. International Drug Price Indicator Guide. [1 December 2015]. (原始内容存档于2017年3月29日). 

参考文献

  • Baldessarini, Ross J.; Frank I. Tarazi. Pharmacotherapy of Psychosis and Mania. Laurence Brunton, John Lazo, Keith Parker (eds.) (编). Goodman & Gilman's The Pharmacological Basis of Therapeutics 11th. New York: McGraw-Hill. 2006. ISBN 978-0071422802. 
  • Bezchlibnyk-Butler, K. Z. Clinical Handbook of Psychotropic Drugs (German Edition)
  • Rote Liste (German Drug Compendium)
  • Benkert, O. and H. Hippius. Psychiatrische Pharmakotherapie (German. 6th Edition, 1996)
  • Physician's Desktop Reference (2004)
  • Heinrich, K. Psychopharmaka in Klinik und Praxis (German, 2nd Edition, 1983)
  • Römpp, Chemielexikon (German, 9th Edition)
  • NINDS Information Homepage (see External links section)
  • Plumb, Dondal C. Plumb's Veterinary Drug Handbook (Blackwell, 5th Edition, 2005)
  • Methods of Execution. Clark County, IN Prosecuting Attorney web page. [2008-08-03]. (原始内容存档于2008-09-14). 

外部链接

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氯丙嗪
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