海洛因:修订间差异

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| protein_bound = 0% ([[吗啡]]代谢产物35%)
| protein_bound = 0% ([[吗啡]]代谢产物35%)
| metabolism = [[肝脏]]
| metabolism = [[肝脏]]
| onset = 几分钟内<ref>{{cite book|last1=Riviello|first1=Ralph J.|title=Manual of forensic emergency medicine : a guide for clinicians|date=2010|publisher=Jones and Bartlett Publishers|location=Sudbury, Mass.|isbn=9780763744625|page=41|url=https://books.google.ca/books?id=keng9ELAE2IC&pg=PA41|access-date=2015-09-03|archive-date=2015-12-08|archive-url=https://web.archive.org/web/20151208002143/https://books.google.ca/books?id=keng9ELAE2IC&pg=PA41|dead-url=no}}</ref>
| onset = 几分钟内<ref>{{cite book|last1=Riviello|first1=Ralph J.|title=Manual of forensic emergency medicine : a guide for clinicians|date=2010|publisher=Jones and Bartlett Publishers|location=Sudbury, Mass.|isbn=9780763744625|page=41||access-date=2015-09-03}}</ref>
| elimination_half-life = 2–3 分钟<ref name=EMC>{{cite web |title=Diamorphine Hydrochloride Injection 30 mg – Summary of Product Characteristics |work=electronic Medicines Compendium |publisher=ViroPharma Limited |date=2013-09-24 |accessdate=2014-03-30 |url=http://www.medicines.org.uk/emc/medicine/28258/SPC/Diamorphine+Hydrochloride+Injection+30+mg/ |deadurl=yes |archiveurl=https://web.archive.org/web/20140330154716/http://www.medicines.org.uk/emc/medicine/28258/SPC/Diamorphine+Hydrochloride+Injection+30+mg/ |archivedate=2014-03-30 }}</ref>
| elimination_half-life = 2–3 分钟<ref name=EMC>{{cite web |title=Diamorphine Hydrochloride Injection 30 mg – Summary of Product Characteristics |work=electronic Medicines Compendium |publisher=ViroPharma Limited |date=2013-09-24 |accessdate=2014-03-30 |url=http://www.medicines.org.uk/emc/medicine/28258/SPC/Diamorphine+Hydrochloride+Injection+30+mg/ }}</ref>
| duration_of_action= 4 至 5 小时<ref>{{cite book |last1=Field |first1=John |title=The Textbook of Emergency Cardiovascular Care and CPR |year=2012 |publisher=Lippincott Williams & Wilkins |isbn=9781469801629 |page=447 |url=https://books.google.ca/books?id=o3m4oNRB4D4C&pg=PA447 |access-date=2015-09-03 |archive-date=2016-03-05 |archive-url=https://web.archive.org/web/20160305040840/https://books.google.ca/books?id=o3m4oNRB4D4C&pg=PA447 |dead-url=no }}</ref>
| duration_of_action= 4 至 5 小时<ref>{{cite book |last1=Field |first1=John |title=The Textbook of Emergency Cardiovascular Care and CPR |year=2012 |publisher=Lippincott Williams & Wilkins |isbn=9781469801629 |page=447 ||access-date=2015-09-03 }}</ref>
| excretion = 90%[[肾脏]]作为{{le|葡萄糖醛酸苷|Glucuronide}},其余为[[胆汁]]
| excretion = 90%[[肾脏]]作为{{le|葡萄糖醛酸苷|Glucuronide}},其余为[[胆汁]]


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<!--Definition and medical uses-->
<!--Definition and medical uses-->
'''海洛因'''({{lang-en|heroin}} 或 {{lang|en|diacetylmorphine}}),俗稱'''白粉'''<ref name="Heroin's rINN">{{cite book|vauthors=Rang HP, Ritter JM, Flower RJ, Henderson G|title=Rang & Dale's Pharmacology|date=2014|publisher=Elsevier Health Sciences|isbn=9780702054976|page=515|edition=8th|url=https://books.google.com/books?id=iOLTBQAAQBAJ&pg=PA515|accessdate=2016-04-12|quote=While 'diamorphine' is the recommended International Nonproprietary Name (rINN), this drug is widely known as heroin.|deadurl=no|archiveurl=https://web.archive.org/web/20210310041413/https://books.google.com/books?id=iOLTBQAAQBAJ&pg=PA515|archivedate=2021-03-10}}</ref>,是一種[[鴉片類藥物|鴉片類毒品]]。
'''海洛因'''({{lang-en|heroin}} 或 {{lang|en|diacetylmorphine}}),俗稱'''白粉'''<ref name="Heroin's rINN">{{cite book|vauthors=Rang HP, Ritter JM, Flower RJ, Henderson G|title=Rang & Dale's Pharmacology|date=2014|publisher=Elsevier Health Sciences|isbn=9780702054976|page=515|edition=8th||accessdate=2016-04-12|quote=While 'diamorphine' is the recommended International Nonproprietary Name (rINN), this drug is widely known as heroin.}}</ref>,是一種[[鴉片類藥物|鴉片類毒品]]。


== 起源 ==
== 起源 ==
在19世纪分析发现[[鸦片]]的药效主要来源于其中的[[生物碱]]、[[可待因]]和[[吗啡]]。1874年,任職英國[[聖瑪麗醫院 (倫敦)|聖瑪莉醫院]]的化學家[[偉特]](C.R Wright)第一次合成海洛因。他把[[嗎啡]]与[[醋酸酐]]加热,得到二乙酰吗啡。該化合物之後送到[[曼徹斯特|曼城]][[曼徹斯特大學|歐文斯學院]]研究。該學院把海洛英注射到[[犬|犬隻]]及[[兔|白兔]]体内,牠們當時出現驚恐、渴睡、瞳孔放大、流大量口水及欲吐的跡象,呼吸最先加速然後紓緩,心跳減弱而不正常等。<ref>{{cite web|url=http://adhpage.dilaudid.net/heroin.html|archiveurl=https://web.archive.org/web/20040606103721/http://adhpage.dilaudid.net/heroin.html|title=eureka...|archivedate=2004-06-06|work=dilaudid.net|deadurl=yes|access-date=2006-06-18}}</ref>偉特并未继续研究该药物。
在19世纪分析发现[[鸦片]]的药效主要来源于其中的[[生物碱]]、[[可待因]]和[[吗啡]]。1874年,任職英國[[聖瑪麗醫院 (倫敦)|聖瑪莉醫院]]的化學家[[偉特]](C.R Wright)第一次合成海洛因。他把[[嗎啡]]与[[醋酸酐]]加热,得到二乙酰吗啡。該化合物之後送到[[曼徹斯特|曼城]][[曼徹斯特大學|歐文斯學院]]研究。該學院把海洛英注射到[[犬|犬隻]]及[[兔|白兔]]体内,牠們當時出現驚恐、渴睡、瞳孔放大、流大量口水及欲吐的跡象,呼吸最先加速然後紓緩,心跳減弱而不正常等。<ref>{{cite web|url=http://adhpage.dilaudid.net/heroin.html||title=eureka...||work=dilaudid.net||access-date=2006-06-18}}</ref>偉特并未继续研究该药物。


1897年,[[德國]][[拜耳公司]]化學家[[菲力克斯·霍夫曼]]再次合成二乙酰吗啡(11日前,他剛成功將[[阿斯匹林]]製成藥物)。他本希望合成[[可待因]]——药效和成瘾性都较小的[[咳藥水]]。海洛英(Heroin)的名字由拜耳藥廠註冊,該字或源自德文heroisch一字,意指[[英雄]],因为海洛因會帶给服用者一种英雄般的感觉。1898年至1910年,海洛因作为一种止咳处方药出售,拜耳公司以「不會上癮的嗎啡」作招徠。當時海洛因極為暢銷,不過由於其處方只是口服極低劑量,故使用者確實沒有發生嚴重成癮問題。但後來發現該藥會在[[肝臟]]中[[代謝]]成嗎啡,而且嗎啡成癮者也改用海洛英,加上拜耳公司曾嘗試隱瞞其危害,令拜耳公司名譽扫地。
1897年,[[德國]][[拜耳公司]]化學家[[菲力克斯·霍夫曼]]再次合成二乙酰吗啡(11日前,他剛成功將[[阿斯匹林]]製成藥物)。他本希望合成[[可待因]]——药效和成瘾性都较小的[[咳藥水]]。海洛英(Heroin)的名字由拜耳藥廠註冊,該字或源自德文heroisch一字,意指[[英雄]],因为海洛因會帶给服用者一种英雄般的感觉。1898年至1910年,海洛因作为一种止咳处方药出售,拜耳公司以「不會上癮的嗎啡」作招徠。當時海洛因極為暢銷,不過由於其處方只是口服極低劑量,故使用者確實沒有發生嚴重成癮問題。但後來發現該藥會在[[肝臟]]中[[代謝]]成嗎啡,而且嗎啡成癮者也改用海洛英,加上拜耳公司曾嘗試隱瞞其危害,令拜耳公司名譽扫地。


== 代谢 ==
== 代谢 ==
口服后,海洛因经过[[首过代谢]],脱去乙酰基,转化为吗啡。<ref name="Sawynok 1986">{{cite journal |author=Sawynok J |title=The therapeutic use of heroin: a review of the pharmacological literature |journal=Can. J. Physiol. Pharmacol. |volume=64 |issue=1 |pages=1–6 |pmid=2420426 |doi= 10.1139/y86-001|url=|date=January 1986}}</ref>如果通过注射,海洛因就可免去[[首过效应]],因为它比吗啡有更强的亲油性,因此可以迅速越过[[血脑屏障]],<ref name="Klous 2005">{{cite journal |last1=Klous |first1=M |last2=Brink |first2=W |last3=Ree |first3=J |last4=Beijnen |first4=J |title=Development of pharmaceutical heroin preparations for medical co-prescription to opioid dependent patients |journal=Drug and Alcohol Dependence |volume=80 |issue=3 |pages=283–95 |year=2005 |pmid=15916865 |doi=10.1016/j.drugalcdep.2005.04.008}}</ref>在大脑之中,它会转化为3-单乙酰吗啡和6-单乙酰吗啡,后者会转化为吗啡,与大脑中的μ-鸦片受体结合,发挥药效。海洛因自身和该受体的结合力弱。<ref>{{cite journal |last1=Inturrisi |first1=C |last2=Schultz |first2=M |last3=Shin |first3=S |last4=Umans |first4=JG |last5=Angel |first5=L |last6=Simon |first6=EJ |title=Evidence from opiate binding studies that heroin acts through its metabolites |journal=Life Sciences |volume=33 |pages=773–6 |year=1983 |pmid=6319928 |doi=10.1016/0024-3205(83)90616-1}}</ref>
口服后,海洛因经过[[首过代谢]],脱去乙酰基,转化为吗啡。<ref name="Sawynok 1986">{{cite journal |author=Sawynok J |title=The therapeutic use of heroin: a review of the pharmacological literature |journal=Can. J. Physiol. Pharmacol. |volume=64 |issue=1 |pages=1–6 |pmid=2420426 |doi= 10.1139/y86-001|url=|date=1986-01}}</ref>如果通过注射,海洛因就可免去[[首过效应]],因为它比吗啡有更强的亲油性,因此可以迅速越过[[血脑屏障]],<ref name="Klous 2005">{{cite journal |last1=Klous |first1=M |last2=Brink |first2=W |last3=Ree |first3=J |last4=Beijnen |first4=J |title=Development of pharmaceutical heroin preparations for medical co-prescription to opioid dependent patients |journal=Drug and Alcohol Dependence |volume=80 |issue=3 |pages=283–95 |year=2005 |pmid=15916865 |doi=10.1016/j.drugalcdep.2005.04.008}}</ref>在大脑之中,它会转化为3-单乙酰吗啡和6-单乙酰吗啡,后者会转化为吗啡,与大脑中的μ-鸦片受体结合,发挥药效。海洛因自身和该受体的结合力弱。<ref>{{cite journal |last1=Inturrisi |first1=C |last2=Schultz |first2=M |last3=Shin |first3=S |last4=Umans |first4=JG |last5=Angel |first5=L |last6=Simon |first6=EJ |title=Evidence from opiate binding studies that heroin acts through its metabolites |journal=Life Sciences |volume=33 |pages=773–6 |year=1983 |pmid=6319928 |doi=10.1016/0024-3205(83)90616-1}}</ref>


== 影響 ==
== 影響 ==