美沙酮

**美沙酮**
系统（IUPAC）命名名称
	(RS)-6-(dimethylamino)-4,4-diphenylheptan-3-one
临床数据
商品名	Dolophine, Methadose, others
Drugs.com	Monograph
MedlinePlus	a682134
妊娠分级	AU: C ; US: C (不排除有风险的可能) ; ;
给药途径	Oral, intravenous, insufflation, sublingual, rectal
合法状态
合法状态	AU: 受管控 (S8) ; CA: Schedule I ; DE: Anlage III ; UK: Class A ; US: Schedule II ; 处方药（℞-only）;
药代动力学数据
生物利用度	41–99% (oral)
蛋白结合度	85–90%
代谢	Liver (CYP3A4, CYP2B6 and CYP2D6-mediated)
开始出现药效	rapid
生物半衰期	7–65 hours
作用时间	4–8 h (one dose), 1–2 days (prolonged use)
排泄	Urine, faeces
识别信息
CAS注册号	76-99-3
ATC代码	N02AC52 N07BC02
PubChem	CID 4095
IUPHAR/BPS	5458
DrugBank	DB00333
ChemSpider	3953
UNII	UC6VBE7V1Z
KEGG	D08195
ChEBI	CHEBI:6807
ChEMBL	CHEMBL651
化学信息
化学式	C21H27NO
摩尔质量	309.445 g/mol
手性	Racemic mixture
	SMILES CCC(C(C1=CC=CC=C1)(C2=CC=CC=C2)CC(N(C)C)C)=O; ;
	InChI InChI=1S/C21H27NO/c1-5-20(23)21(16-17(2)22(3)4,18-12-8-6-9-13-18)19-14-10-7-11-15-19/h6-15,17H,5,16H2,1-4H3 ; Key:USSIQXCVUWKGNF-UHFFFAOYSA-N ;

美沙酮（拉丁语：Methadone，或翻译为美沙冬）商用名包括多罗芬（拉丁语：Dolophine），是一种鸦片类药物。适用于缓解疼痛以及维持治疗，或用于帮助戒毒人士摆脱鸦片依赖^[3]。戒毒治疗可在不到一个月的时间内迅速完成，亦可在不到六个月的时间内逐渐完成。美沙酮单次剂量使用后作用迅速，但需持续使用五天才可达至最大效果。单次剂量使用后药效可持续约六小时，长期使用时单次剂量使用效果可持续一天半左右。美沙酮一般可通过口服、肌肉注射或静脉注射使用^[3]。

美沙酮的副作用和其他类鸦片麻醉药相似，常见的包括有晕眩、嗜睡、呕吐与盗汗。较严重的副作用则像是滥用及呼吸困难。其他如心律不整包括长QT症等症状都有可能发生^[3]。根据2011年美国国内统计，由于麻醉药使用过量而造成的死亡人数中，有26%（大约是4,418人）死于美沙酮中毒^[4]，使用剂量越高则有越高的几率会有副作用产生的风险^[5]。美沙酮是经由化学合成且其机转是借着结合类鸦片受体以达到止痛效用^[3]。

美沙酮大约在1937年至1939年间由古斯塔夫·爱哈特和麦克斯·勃克穆尔两人在德国合成并问世^[6]^[7]，于1947年被美国认可且在国内使用^[3]。美沙酮是世界卫生组织基本药物标准清单内的药物，同时更为基础医疗系统内的重要必须药品^[8]。2013年，全球共生产美沙酮约41,400公斤，它的使用规范和一般麻醉药物相同^[9]^[10]。在美国当地，美沙酮并不是十分昂贵的药品^[11]。

美沙酮现在主要是用来作为海洛因的代替品，用以治疗有使用海洛因习惯的毒品使用者。“美沙酮治疗法”是现时治疗海洛因毒患的可靠办法。

参考

↑ ^1.0 ^1.1 ^1.2 Fredheim, OM; Moksnes, K; Borchgrevink, PC; Kaasa, S; Dale, O. Clinical pharmacology of methadone for pain.. Acta Anaesthesiologica Scandinavica. 2008-08, 52 (7): 879–89. PMID 18331375. doi:10.1111/j.1399-6576.2008.01597.x.
↑ ^2.0 ^2.1 ^2.2 Brown, R; Kraus, C; Fleming, M; Reddy, S. Methadone: applied pharmacology and use as adjunctive treatment in chronic pain. (PDF). Postgraduate Medical Journal. 2004-11, 80 (949): 654–9 [2016-09-27]. PMC 1743125 . PMID 15537850. doi:10.1136/pgmj.2004.022988.
↑ ^3.0 ^3.1 ^3.2 ^3.3 ^3.4 ^3.5 ^3.6 Methadone Hydrochloride. The American Society of Health-System Pharmacists. [Dec 2015].
↑ Data table for Figure 1. Age-adjusted drug-poisoning and opioid-analgesic poisoning death rates: United States, 1999–2011 (PDF). CDC. [2015-12-22].
↑ Chou, R; Turner, JA; Devine, EB; Hansen, RN; Sullivan, SD; Blazina, I; Dana, T; Bougatsos, C; Deyo, RA. The effectiveness and risks of long-term opioid therapy for chronic pain: a systematic review for a National Institutes of Health Pathways to Prevention Workshop.. Annals of Internal Medicine. 2015-02-17, 162 (4): 276–86. PMID 25581257. doi:10.7326/M14-2559.
↑ Methadone Matters: Evolving Community Methadone Treatment of Opiate Addiction. CRC Press. 2003: 13. ISBN 9780203633090.
↑ Diphenypropylamine Derivatives. Encyclopedia of Drug Policy. 2011. ISBN 9781506338248.
↑ WHO Model List of EssentialMedicines (PDF). World Health Organization. 2013-10 [2014-04-22].
↑ Narcotic Drugs 2014 (pdf). INTERNATIONAL NARCOTICS CONTROL BOARD. 2015: 21 [2016-09-27]. ISBN 9789210481571.
↑ Organization, World Health. Guidelines for the psychosocially assisted pharmacological treatment of opioid dependence.. Geneva: World Health Organization. 2009: 78. ISBN 9789241547543.
↑ Hamilton, Richart. Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. 2015: 13. ISBN 9781284057560.

[acta08-1] 1.0 ^1.1 ^1.2 Fredheim, OM; Moksnes, K; Borchgrevink, PC; Kaasa, S; Dale, O. Clinical pharmacology of methadone for pain.. Acta Anaesthesiologica Scandinavica. 2008-08, 52 (7): 879–89. PMID 18331375. doi:10.1111/j.1399-6576.2008.01597.x.

[PMJ04-2] 2.0 ^2.1 ^2.2 Brown, R; Kraus, C; Fleming, M; Reddy, S. Methadone: applied pharmacology and use as adjunctive treatment in chronic pain. (PDF). Postgraduate Medical Journal. 2004-11, 80 (949): 654–9 [2016-09-27]. PMC 1743125 . PMID 15537850. doi:10.1136/pgmj.2004.022988.

[AHFS2015-3] 3.0 ^3.1 ^3.2 ^3.3 ^3.4 ^3.5 ^3.6 Methadone Hydrochloride. The American Society of Health-System Pharmacists. [Dec 2015].

[4] Data table for Figure 1. Age-adjusted drug-poisoning and opioid-analgesic poisoning death rates: United States, 1999–2011 (PDF). CDC. [2015-12-22].

[5] Chou, R; Turner, JA; Devine, EB; Hansen, RN; Sullivan, SD; Blazina, I; Dana, T; Bougatsos, C; Deyo, RA. The effectiveness and risks of long-term opioid therapy for chronic pain: a systematic review for a National Institutes of Health Pathways to Prevention Workshop.. Annals of Internal Medicine. 2015-02-17, 162 (4): 276–86. PMID 25581257. doi:10.7326/M14-2559.

[6] Methadone Matters: Evolving Community Methadone Treatment of Opiate Addiction. CRC Press. 2003: 13. ISBN 9780203633090.

[7] Diphenypropylamine Derivatives. Encyclopedia of Drug Policy. 2011. ISBN 9781506338248.

[8] WHO Model List of EssentialMedicines (PDF). World Health Organization. 2013-10 [2014-04-22].

[UN2015-9] Narcotic Drugs 2014 (pdf). INTERNATIONAL NARCOTICS CONTROL BOARD. 2015: 21 [2016-09-27]. ISBN 9789210481571.

[10] Organization, World Health. Guidelines for the psychosocially assisted pharmacological treatment of opioid dependence.. Geneva: World Health Organization. 2009: 78. ISBN 9789241547543.

[Ric2015-11] Hamilton, Richart. Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. 2015: 13. ISBN 9781284057560.

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