美沙酮

**美沙酮**
系統（IUPAC）命名名稱
	(RS)-6-(dimethylamino)-4,4-diphenylheptan-3-one
臨床數據
商品名	Dolophine, Methadose, others
Drugs.com	Monograph
MedlinePlus	a682134
妊娠分級	AU: C ; US: C (不排除有風險的可能) ; ;
給藥途徑	Oral, intravenous, insufflation, sublingual, rectal
合法狀態
合法狀態	AU: 受管控 (S8) ; CA: Schedule I ; DE: Anlage III ; UK: Class A ; US: Schedule II ; 處方藥（℞-only）;
藥代動力學數據
生物利用度	41–99% (oral)
蛋白結合度	85–90%
代謝	Liver (CYP3A4, CYP2B6 and CYP2D6-mediated)
開始出現藥效	rapid
生物半衰期	7–65 hours
作用時間	4–8 h (one dose), 1–2 days (prolonged use)
排泄	Urine, faeces
識別資訊
CAS註冊號	76-99-3
ATC代碼	N02AC52 N07BC02
PubChem	CID 4095
IUPHAR/BPS	5458
DrugBank	DB00333
ChemSpider	3953
UNII	UC6VBE7V1Z
KEGG	D08195
ChEBI	CHEBI:6807
ChEMBL	CHEMBL651
化學資訊
化學式	C21H27NO
摩爾質量	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（拉丁語：Methadone，或翻譯為美沙冬）商用名包括多羅芬（拉丁語：Dolophine），是一種鴉片類藥物。適用於緩解疼痛以及維持治療，或用於幫助戒毒人士擺脫鴉片依賴^[3]。戒毒治療可在不到一個月的時間內迅速完成，亦可在不到六個月的時間內逐漸完成。美沙酮單次劑量使用後作用迅速，但需持續使用五天才可達至最大效果。單次劑量使用後藥效可持續約六小時，長期使用時單次劑量使用效果可持續一天半左右。美沙酮一般可通過口服、肌肉注射或靜脈注射使用^[3]。

美沙酮的副作用和其他類鴉片麻醉藥相似，常見的包括有暈眩、嗜睡、嘔吐與盜汗。較嚴重的副作用則像是濫用及呼吸困難。其他如心律不整包括長QT症等症狀都有可能發生^[3]。根據2011年美國國內統計，由於麻醉藥使用過量而造成的死亡人數中，有26%（大約是4,418人）死於美沙酮中毒^[4]，使用劑量越高則有越高的概率會有副作用產生的風險^[5]。美沙酮是經由化學合成且其機轉是藉着結合類鴉片受體以達到止痛效用^[3]。

美沙酮大約在1937年至1939年間由古斯塔夫·愛哈特和麥克斯·勃克穆爾兩人在德國合成並問世^[6]^[7]，於1947年被美國認可且在國內使用^[3]。美沙酮是世界衛生組織基本藥物標準清單內的藥物，同時更為基礎醫療系統內的重要必須藥品^[8]。2013年，全球共生產美沙酮約41,400公斤，它的使用規範和一般麻醉藥物相同^[9]^[10]。在美國當地，美沙酮並不是十分昂貴的藥品^[11]。

美沙酮現在主要是用來作為海洛英的代替品，用以治療有使用海洛英習慣的毒品使用者。「美沙酮治療法」是現時治療海洛英毒患的可靠辦法。

參考

↑ ^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.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]

[9]

[10]

[11]