氯丙嗪:修订间差异
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{{medical}} |
{{medical}} |
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{{Drugbox| Watchedfields = changed |
{{Drugbox |
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| Watchedfields = changed |
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| verifiedrevid = |
| verifiedrevid = 443519547 |
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| IUPAC_name = 3-(2-chloro-10''H''-phenothiazin-10-yl)-''N'',''N''-dimethyl-propan-1-amine |
| IUPAC_name = 3-(2-chloro-10''H''-phenothiazin-10-yl)-''N'',''N''-dimethyl-propan-1-amine |
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| image = Chlorpromazine |
| image = Chlorpromazine.svg |
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| alt = Skeletal formula of chlorpromazine |
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| width = 222 |
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| image2 = Chlorpromazine-3D-balls.png |
| image2 = Chlorpromazine-3D-balls.png |
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| alt2 = Ball-and-stick model of the chlorpromazine molecule |
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| CASNo_Ref = {{cascite}} |
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<!--Clinical data--> |
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| tradename = Largactil, Thorazine, others |
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| smiles = Clc2cc1N(c3c(Sc1cc2)cccc3)CCCN(C)C |
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| Drugs.com = {{drugs.com|monograph|chlorpromazine-hydrochloride}} |
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| MedlinePlus = a682040 |
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| pregnancy_AU = C |
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| pregnancy_US = C |
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| legal_AU = S4 |
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| legal_CN = 处方药 |
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| legal_CA = Rx-only |
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| legal_UK = POM |
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| legal_US = Rx-only |
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<!--Pharmacokinetic data--> |
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| bioavailability = 10–80%(口服,視體質而定)<ref name=TGA>{{cite web|title=PRODUCT INFORMATION LARGACTIL|work=TGA eBusiness Services|publisher=Sanofi Aventis Pty Ltd|date=28 August 2012|accessdate=8 December 2013|url=https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/pdf?OpenAgent&id=CP-2010-PI-05882-3|format=PDF|deadurl=no|archiveurl=https://web.archive.org/web/20170330162812/https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/pdf?OpenAgent&id=CP-2010-PI-05882-3|archivedate=30 March 2017}}</ref> |
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| protein_bound = 90–99%<ref name = TGA/> |
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| elimination_half-life = 30 小時<ref name=AHFS2015/> |
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| excretion = 尿液(24小時內排除43–65%)<ref name = TGA/> |
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<!--Identifiers--> |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number = 50-53-3 |
| CAS_number = 50-53-3 |
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| CAS_number_comment = 自由基團 |
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| CAS_supplemental = (自由基)<br/>{{CAS|69-09-0}} (有機鹽酸鹽) |
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| |
| CAS_number2 = 69-09-0 |
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| CAS_number2_comment = 鹽酸鹽 |
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| ATC_prefix = N05 |
| ATC_prefix = N05 |
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| ATC_suffix = AA01 |
| ATC_suffix = AA01 |
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| ATC_supplemental = |
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| PubChem = 2726 |
| PubChem = 2726 |
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| IUPHAR_ligand = 83 |
| IUPHAR_ligand = 83 |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank = DB00477 |
| DrugBank = DB00477 |
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} |
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| ChemSpiderID = 2625 |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| bioavailability = Oral, 30 to 50% (interindividual variations 10–70%) |
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| UNII = U42B7VYA4P |
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| KEGG_Ref = {{keggcite|correct|kegg}} |
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| elimination_half-life = 16 to 30 hours. In long term treatment, CPZ induces its own metabolism |
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| KEGG = D00270 |
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| excretion = Biliary and [[kidney|renal]], as metabolites (only traces of unchanged drug) |
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| ChEBI_Ref = {{ebicite|correct|EBI}} |
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| pregnancy_category = C—only when benefit for the mother exceeds risk to unborn child |
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| |
| ChEBI = 3647 |
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| ChEMBL_Ref = {{ebicite|correct|EBI}} |
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| ChEMBL = 71 |
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<!--Chemical data--> |
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| smiles = CN(C)CCCN1c2ccccc2Sc3c1cc(cc3)Cl |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} |
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}} |
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<!-- Definition and medical uses --> |
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'''氯丙嗪'''(Chlorpromazine,簡稱'''CPZ'''),常見商標名 '''Thorazine''' 或 '''Largactil''',是一種[[抗精神病药|精神科藥物]]<ref name=AHFS2015/>。本品一般用於治療[[精神分裂症]]等[[思覺失調]]<ref name=AHFS2015/>。其他用途還可用做作治療[[躁鬱症]]、[[注意力不足過動症|過動症]]、[[恶心]]、[[呕吐]]、術前焦慮,或是其他方法無法控制的[[打嗝]]症狀等等<ref name=AHFS2015/>。本品可以口服、[[肌肉注射]]或[[靜脈注射]]<ref name=AHFS2015/>。 |
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'''氯丙嗪'''(Chlorpromazine、CPZ,[[美國]]:Thorazine,其它地區:Largactil),也叫冬眠灵,是第一个抗精神病药,开创了药物治疗精神疾病的历史。从1950年代初氯丙嗪用于治疗[[精神分裂]]症和[[躁狂]]症开始,进入了精神药理学发展的黄金阶段。氯丙嗪的发现改变了精神分裂症患者的预后,並在西方国家掀起了[[非住院化运动]],使许多精神病患者不必被终身强迫关锁在医院裡。氯丙嗪的发现具有里程碑式的意义。 |
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<!-- Side effects and mechanism--> |
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常見副作用包含[[錐體外症候群]]、[[鎮靜|嗜睡]]、口乾、[[姿位性低血壓]],以及體重增加等等<ref name=AHFS2015/>。嚴重副作用可能導致{{tsl|en|tardive dyskinesia|遲發性不自主運動}}等永久運動功能障礙、{{tsl|en|neuroleptic malignant syndrome|抗精神藥物惡性症候群}}、以及[[白细胞减少症]]<ref name=AHFS2015/>。因[[失智症]]導致精神錯亂的老年人用藥可能會增加死亡風險<ref name=AHFS2015/>。[[妊娠]]期間用藥的安全性迄今不明<ref name=AHFS2015/>。本品屬於{{tsl|en|typical antipsychotic|典型抗憂鬱藥物}}<ref name=AHFS2015/>。其作用機制尚未明朗,但可能與其具{{tsl|en|dopamine antagonist|多巴胺受體拮抗劑|}}的活性有關<ref name=AHFS2015/>。本品亦具有{{tsl|en|antiserotonergic|抗血清素活性|抗血清素}}以及[[抗組織胺藥|抗組織胺]]的活性<ref name="AHFS2015">{{cite web|url=http://www.drugs.com/monograph/chlorpromazine-hydrochloride.html|title=Chlorpromazine Hydrochloride|accessdate=Dec 1, 2015|author=|date=|publisher=The American Society of Health-System Pharmacists|archiveurl=https://web.archive.org/web/20151208163938/http://www.drugs.com/monograph/chlorpromazine-hydrochloride.html|archivedate=8 December 2015|deadurl=no}}</ref>。 |
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<!-- History, society and culture --> |
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本品最早於1950年發現,為第一種精神疾患藥物<ref name="history05">{{Cite journal|doi=10.1080/10401230591002002|last1=López-Muñoz |first1=Francisco |last2=Alamo |first2=Cecilio |last3=Cuenca|first3=Eduardo|last4=Shen |first4=Winston W. |last5=Clervoy |first5=Patrick |last6=Rubio |first6=Gabriel |year=2005 |title=History of the discovery and clinical introduction of chlorpromazine |journal=Annals of Clinical Psychiatry |volume=17 |issue=3|pages=113–35|pmid=16433053}}</ref><ref name=Ban2007>{{cite journal|last1=Ban|first1=TA|title=Fifty years chlorpromazine: a historical perspective.|journal=Neuropsychiatric disease and treatment|date=August 2007|volume=3|issue=4|pages=495–500|pmid=19300578|pmc=2655089}}</ref>。本品列名於[[世界卫生组织基本药物标准清单]]之中,為基礎公衛體系必備藥物之一<ref name=WHO19th>{{cite web|title=WHO Model List of Essential Medicines (19th List)|url=http://www.who.int/medicines/publications/essentialmedicines/EML_2015_FINAL_amended_NOV2015.pdf?ua=1|work=World Health Organization|accessdate=8 December 2016|date=April 2015|deadurl=no|archiveurl=https://web.archive.org/web/20161213052708/http://www.who.int/medicines/publications/essentialmedicines/EML_2015_FINAL_amended_NOV2015.pdf?ua=1|archivedate=13 December 2016}}</ref>。氯丙嗪的發現為精神醫療的{{tsl|en|history of psychiatry|精神醫學歷史|重大里程碑}}<ref>{{cite journal|last1=López-Muñoz|first1=F|last2=Alamo|first2=C|last3=Cuenca|first3=E|last4=Shen|first4=WW|last5=Clervoy|first5=P|last6=Rubio|first6=G|title=History of the discovery and clinical introduction of chlorpromazine.|journal=Annals of Clinical Psychiatry|date=2005|volume=17|issue=3|pages=113–35|pmid=16433053|doi=10.1080/10401230591002002}}</ref><ref>{{cite book|last1=Shorter|first1=Edward|title=A historical dictionary of psychiatry|date=2005|publisher=Oxford University Press|location=New York|isbn=9780198039235|page=6|url=https://books.google.com/books?id=M49pEDoEpl0C&pg=PA6|deadurl=no|archiveurl=https://web.archive.org/web/20170214213428/https://books.google.com/books?id=M49pEDoEpl0C&pg=PA6|archivedate=14 February 2017}}</ref>。本品屬於[[通用名藥物]]<ref name=AHFS2015/>,其於[[開發中國家]]的每日劑量批發價約介於 0.02 至 0.12 美金之間<ref>{{cite web|title=Chlorpromazine HCL|url=http://erc.msh.org/dmpguide/resultsdetail.cfm?language=english&code=CPZ100T&s_year=2014&year=2014&str=100%20mg&desc=Chlorpromazine%20HCl&pack=new&frm=TAB-CAP&rte=PO&class_code2=24%2E1%2E&supplement=&class_name=%2824%2E1%2E%29Medicines%20used%20in%20psychotic%20disorders%3Cbr%3E|website=International Drug Price Indicator Guide|accessdate=1 December 2015|deadurl=yes|archiveurl=https://web.archive.org/web/20170329013315/http://erc.msh.org/dmpguide/resultsdetail.cfm?language=english&code=CPZ100T&s_year=2014&year=2014&str=100%20mg&desc=Chlorpromazine%20HCl&pack=new&frm=TAB-CAP&rte=PO&class_code2=24.1.&supplement=&class_name=%2824.1.%29Medicines%20used%20in%20psychotic%20disorders%3Cbr%3E|archivedate=2017年3月29日}}</ref>。在美國同樣劑量則約需 2 美金<ref name=AHFS2015/>。 |
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==藥理學== |
==藥理學== |
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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。 |
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。 |
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==不良反應== |
==不良反應== |
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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。 |
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]]。 |
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==劑型及用量== |
==劑型及用量== |
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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[[鹽酸異丙嗪]](也叫非那根)合用,组成冬非合剂。 |
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[[鹽酸異丙嗪]](也叫非那根)合用,组成冬非合剂。 |
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==註釋== |
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{{reflist|2}} |
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==參考文獻== |
==參考文獻== |
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{{refbegin| |
{{refbegin|2}} |
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*{{cite book |last=Baldessarini |first=Ross J. |coauthors=Frank I. Tarazi |editor=Laurence Brunton, John Lazo, Keith Parker (eds.) |title=[[Goodman & Gilman's The Pharmacological Basis of Therapeutics]] |edition=11<sup>th</sup> |year=2006 |publisher=[[McGraw-Hill]] |location=New York |isbn=978-0071422802|pages= |chapter=Pharmacotherapy of Psychosis and Mania }} |
*{{cite book |last=Baldessarini |first=Ross J. |coauthors=Frank I. Tarazi |editor=Laurence Brunton, John Lazo, Keith Parker (eds.) |title=[[Goodman & Gilman's The Pharmacological Basis of Therapeutics]] |edition=11<sup>th</sup> |year=2006 |publisher=[[McGraw-Hill]] |location=New York |isbn=978-0071422802|pages= |chapter=Pharmacotherapy of Psychosis and Mania }} |
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*Bezchlibnyk-Butler, K. Z. ''Clinical Handbook of Psychotropic Drugs'' (German Edition) |
*Bezchlibnyk-Butler, K. Z. ''Clinical Handbook of Psychotropic Drugs'' (German Edition) |
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*NINDS Information Homepage (see External links section) |
*NINDS Information Homepage (see External links section) |
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*Plumb, Dondal C. ''Plumb's Veterinary Drug Handbook'' (Blackwell, 5th Edition, 2005) |
*Plumb, Dondal C. ''Plumb's Veterinary Drug Handbook'' (Blackwell, 5th Edition, 2005) |
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*{{cite web |url=http://www.clarkprosecutor.org/html/death/methods.htm |title=Methods of Execution |accessdate=2008-08-03 |work=Clark County, IN Prosecuting Attorney web page}} |
*{{cite web |url=http://www.clarkprosecutor.org/html/death/methods.htm |title=Methods of Execution |accessdate=2008-08-03 |work=Clark County, IN Prosecuting Attorney web page |archive-date=2008-09-14 |archive-url=https://web.archive.org/web/20080914164956/http://www.clarkprosecutor.org/html/death/methods.htm |dead-url=no }} |
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{{refend}} |
{{refend}} |
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==外部連結== |
==外部連結== |
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* [http://www.nlm.nih.gov/medlineplus/druginfo/meds/a682040.html Medlineplus article on chlorpromazine] |
* [http://www.nlm.nih.gov/medlineplus/druginfo/meds/a682040.html Medlineplus article on chlorpromazine] {{Wayback|url=http://www.nlm.nih.gov/medlineplus/druginfo/meds/a682040.html |date=20100615175522 }} |
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* [http://www.ninds.nih.gov/disorders/tardive/tardive.htm National Institute of Neurological Disorders and Stroke (NINDS) Tardive Dyskinesia information page] |
* [http://www.ninds.nih.gov/disorders/tardive/tardive.htm National Institute of Neurological Disorders and Stroke (NINDS) Tardive Dyskinesia information page] {{Wayback|url=http://www.ninds.nih.gov/disorders/tardive/tardive.htm |date=20120427104252 }} |
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* [http://druginfo.nlm.nih.gov/drugportal/dpdirect.jsp?name=Chlorpromazine U.S. National Library of Medicine: Drug Information Portal - Chlorpromazine] |
* [http://druginfo.nlm.nih.gov/drugportal/dpdirect.jsp?name=Chlorpromazine U.S. National Library of Medicine: Drug Information Portal - Chlorpromazine] {{Wayback|url=http://druginfo.nlm.nih.gov/drugportal/dpdirect.jsp?name=Chlorpromazine |date=20100615040949 }} |
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{{止吐剂}} |
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{{Sigmaergics}} |
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{{Hypnotics and sedatives}} |
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{{异生素敏感受体调节剂}} |
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[[bg:Хлорпромазин]] |
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[[Category:世界卫生组织基本药物]] |
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[[de:Chlorpromazin]] |
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[[Category:肝毒素]] |
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[[Category:CYP2D6抑制剂]] |
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[[es:Clorpromazina]] |
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[[Category:α2受体拮抗剂]] |
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[[fi:Klooripromatsiini]] |
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[[fr:Chlorpromazine]] |
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[[he:כלורפרומאזין]] |
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[[hu:Klórpromazin]] |
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[[it:Clorpromazina]] |
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[[ja:クロルプロマジン]] |
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[[nl:Chloorpromazine]] |
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[[pl:Chlorpromazyna]] |
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[[pt:Clorpromazina]] |
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[[ru:Хлорпромазин]] |
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[[simple:Chlorpromazine]] |
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[[sr:Ларгактил]] |
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[[sv:Klorpromazin]] |
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[[tr:Klorpromazin]] |
2024年6月30日 (日) 04:07的最新版本
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臨床資料 | |
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商品名 | Largactil, Thorazine, others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682040 |
核准狀況 | |
懷孕分級 |
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给药途径 | 口服(藥丸或糖漿)、肛門塞劑、肌肉注射、靜脈注射 |
ATC碼 | |
法律規範狀態 | |
法律規範 |
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藥物動力學數據 | |
生物利用度 | 10–80%(口服,視體質而定)[1] |
血漿蛋白結合率 | 90–99%[1] |
药物代谢 | 肝臟,大多經CYP2D6[1] |
生物半衰期 | 30 小時[2] |
排泄途徑 | 尿液(24小時內排除43–65%)[1] |
识别信息 | |
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CAS号 | 50-53-3(自由基團) ![]() 69-09-0(鹽酸鹽) |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.000.042 |
化学信息 | |
化学式 | C17H19ClN2S |
摩尔质量 | 318.86 g/mol(自由基團) 355.33 g/mol(鹽酸鹽) |
3D模型(JSmol) | |
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氯丙嗪(Chlorpromazine,簡稱CPZ),常見商標名 Thorazine 或 Largactil,是一種精神科藥物[2]。本品一般用於治療精神分裂症等思覺失調[2]。其他用途還可用做作治療躁鬱症、過動症、恶心、呕吐、術前焦慮,或是其他方法無法控制的打嗝症狀等等[2]。本品可以口服、肌肉注射或靜脈注射[2]。
常見副作用包含錐體外症候群、嗜睡、口乾、姿位性低血壓,以及體重增加等等[2]。嚴重副作用可能導致遲發性不自主運動等永久運動功能障礙、抗精神藥物惡性症候群、以及白细胞减少症[2]。因失智症導致精神錯亂的老年人用藥可能會增加死亡風險[2]。妊娠期間用藥的安全性迄今不明[2]。本品屬於典型抗憂鬱藥物[2]。其作用機制尚未明朗,但可能與其具多巴胺受體拮抗劑的活性有關[2]。本品亦具有抗血清素以及抗組織胺的活性[2]。
本品最早於1950年發現,為第一種精神疾患藥物[3][4]。本品列名於世界卫生组织基本药物标准清单之中,為基礎公衛體系必備藥物之一[5]。氯丙嗪的發現為精神醫療的重大里程碑[6][7]。本品屬於通用名藥物[2],其於開發中國家的每日劑量批發價約介於 0.02 至 0.12 美金之間[8]。在美國同樣劑量則約需 2 美金[2]。
藥理學
[编辑]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。
不良反應
[编辑]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。
劑型及用量
[编辑]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,另外针剂通常与鹽酸異丙嗪(也叫非那根)合用,组成冬非合剂。
註釋
[编辑]- ^ 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).
- ^ 2.00 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).
- ^ 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.
- ^ Ban, TA. Fifty years chlorpromazine: a historical perspective.. Neuropsychiatric disease and treatment. August 2007, 3 (4): 495–500. PMC 2655089
. PMID 19300578.
- ^ 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).
- ^ 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.
- ^ 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).
- ^ Chlorpromazine HCL. International Drug Price Indicator Guide. [1 December 2015]. (原始内容存档于2017年3月29日).
參考文獻
[编辑]- 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).
外部連結
[编辑]- Medlineplus article on chlorpromazine (页面存档备份,存于互联网档案馆)
- National Institute of Neurological Disorders and Stroke (NINDS) Tardive Dyskinesia information page (页面存档备份,存于互联网档案馆)
- U.S. National Library of Medicine: Drug Information Portal - Chlorpromazine (页面存档备份,存于互联网档案馆)
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