阿米替林

**阿米替林**
臨床資料
商品名	Amitrip, Elevil, Endep, Levate
AHFS/Drugs.com	Monograph
MedlinePlus	a682388
核准狀況	美 FDA: Amitriptyline;
懷孕分級	澳: C ;
给药途径	口服，肌注
ATC碼	N06AA09 (WHO) ;
法律規範狀態
法律規範	澳：限医生处方（S4）; 加：处方药（℞-only）; 英：处方药（℞-only） (POM); 美：处方药（℞-only）;
藥物動力學數據
生物利用度	30–60%因经过首过代谢
血漿蛋白結合率	96%[1][2][3][4]
药物代谢	肝脏 (CYP2D6)[1][2][3][4]
生物半衰期	22.4 小时(26 hr for active metabolite, nortriptyline)[1][2][3][4]
排泄途徑	肾脏[1][2][3][4]
识别
	IUPAC命名法 3-(10,11-Dihydro-5H-dibenzo[a,d]cycloheptene-5-ylidene)-N,N-dimethylpropan-1-amine; ;
CAS号	50-48-6 ; 549-18-8（hydrochloride）
PubChem CID	2160;
IUPHAR/BPS	200;
DrugBank	DB00321 ;
ChemSpider	2075 ;
UNII	1806D8D52K;
KEGG	D07448 ;
ChEBI	CHEBI:2666 ;
ChEMBL	ChEMBL629 ;
CompTox Dashboard (EPA)	DTXSID7022594 ;
ECHA InfoCard	100.000.038
化学
化学式	C20H23N
摩尔质量	277.403 g/mol
3D模型（JSmol）	交互式图像;
	SMILES c3cc2c(/C(c1c(cccc1)CC2)=C\CCN(C)C)cc3;
	InChI InChI=1S/C20H23N/c1-21(2)15-7-12-20-18-10-5-3-8-16(18)13-14-17-9-4-6-11-19(17)20/h3-6,8-12H,7,13-15H2,1-2H3 ; Key:KRMDCWKBEZIMAB-UHFFFAOYSA-N ;

阿米替林（）[5]，商品名稱Elavil，是使用最广泛的一种止痛药。[6] 阿米替林可以治疗许多精神障碍[7]，包括重度抑郁症和焦虑症，有时候也用来治疗精神病、注意力缺陷多动障碍（ADHD，多动症）和双相情感障碍[7][8]。阿米替林也可以預防偏头痛、治療包括纖維肌痛症及疱疹後神經痛在内的神經性疼痛，偶爾也會被用於治療失眠[7][9]。該藥屬於口服藥物[7]。

常見的副作用包含口乾、視覺障礙、姿位性低血壓、嗜睡，以及便秘等等。嚴重的副作用可能會造成癲癇發作、尿滯留、青光眼，或是其他心臟問題，25歲以下的用藥者甚至會有增加自殺念頭的風險。該藥切忌與单胺氧化酶抑制剂或希塞菩等藥物合用[7]。妊娠時服用阿米替林可能具有風險[10][7]，哺乳期間用藥目前認為是安全的[11]。該藥為使用最廣泛的一種三環類抗抑鬱藥（TCA），然其詳細機轉仍不清楚[7]。

在1960年首次發現阿米替林[12]，並於1961年被美國食品藥品監督管理局核准[13]。該藥列名世界衛生組織基本藥物標準清單當中，為基礎醫療體系的必備用藥之一[14]。該藥屬於通用名藥物[7]，2014年每劑的批發價價格區間位於0.01至0.04美金之間[15]，美國境內則約一劑0.20美金左右[7]。

药理

药效

受体	K_i [nM][lower-alpha 1] (阿米替林)[16][17]	K_i [nM][lower-alpha 2] (去甲替林)[16][17]
SERT	3.13	16.5
NET	22.4	4.37
DAT	5380	3100
5-HT_1A	450	294
5-HT_1B	840	-
5-HT_2A	4.3	5
5-HT_2C	6.15	8.5
5-HT₆	103	148
5-HT₇	114	-
H₁	1.1	15.1
H₃	1000	-
H₄	33.6	-
M₁	12.9	40
M₂	11.8	110
M₃	25.9	50
M₄	7.2	84
M₅	19.9	97
α₁	24	55
α₂	690	2030
D₁	89	-
D₂	1460	2570
D₃	206	-
D₅	170	-
σ	300	2000

備註

These K_i values are averaged binding affinities towards cloned human receptors when available.
As with amitriptyline, these K_ivalues are averaged binding affinities towards cloned human receptors when available.

引用

. DailyMed. Dispensing Solutions, Inc. September 2013 [1 December 2013]. （原始内容存档于2013-12-03）.
. Medscape Reference. WebMD. [1 December 2013]. （原始内容存档于2013-12-03）.
(PDF). TGA eBusiness Services. Alphapharm Pty Limited. 10 December 2012 [1 December 2013]. （原始内容存档于2017-08-13）.
. electronic Medicines Compendium. Actavis UK Ltd. 24 March 2013 [1 December 2013]. （原始内容存档于2013-12-03）.
. [2015-09-26]. （原始内容存档于2014-07-14）.
A.S. Yazdi, N. Razavi, S.R. Yazdinejad. Separation and determination of amitriptyline and nortriptyline by dispersive liquid–liquid microextraction combined with gas chromatography flame ionization detection. Talanta, 75 (2008), pp. 1293–1299
. The American Society of Health-System Pharmacists. [Sep 25, 2014]. （原始内容存档于2014-09-24）.
Leucht, C; Huhn, M; Leucht, S. . The Cochrane Database of Systematic Reviews. December 2012, 12: CD009138. PMID 23235671. doi:10.1002/14651858.CD009138.pub2.
Moore, RA; Derry, S; Aldington, D; Cole, P; Wiffen, PJ. . The Cochrane database of systematic reviews. 6 July 2015, 7: CD008242. PMID 26146793.
. Australian Government. 3 March 2014 [22 April 2014]. （原始内容存档于2014-04-08）.
. drugs.com. Sep 8, 2014 [25 September 2014]. （原始内容存档于2014-09-24）.
Sneader, Walter. . Chichester: John Wiley & Sons. 2005: 414. ISBN 9780470015520.
Fangmann P, Assion HJ, Juckel G, González CA, López-Muñoz F. . Journal of Clinical Psychopharmacology. February 2008, 28 (1): 1–4. PMID 18204333. doi:10.1097/jcp.0b013e3181627b60.
(PDF). World Health Organization. October 2013 [22 April 2014]. （原始内容存档 (PDF)于2014-04-23）.
. International Drug Price Indicator Guide. [2 December 2015]. （原始内容存档于2017年3月30日）.
Roth, BL; Driscol, J. . Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. 12 January 2011 [1 December 2013]. （原始内容存档于2013-11-08）.
Brunton, L; Chabner, B; Knollman, B. 12th. New York: McGraw-Hill Professional. 2010. ISBN 978-0-07-162442-8.

This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.

[16] These K_i values are averaged binding affinities towards cloned human receptors when available.

[19] As with amitriptyline, these K_ivalues are averaged binding affinities towards cloned human receptors when available.

[DM-1] . DailyMed. Dispensing Solutions, Inc. September 2013 [1 December 2013]. （原始内容存档于2013-12-03）.

[MSR-2] . Medscape Reference. WebMD. [1 December 2013]. （原始内容存档于2013-12-03）.

[TGA-3] (PDF). TGA eBusiness Services. Alphapharm Pty Limited. 10 December 2012 [1 December 2013]. （原始内容存档于2017-08-13）.

[EMC-4] . electronic Medicines Compendium. Actavis UK Ltd. 24 March 2013 [1 December 2013]. （原始内容存档于2013-12-03）.

[5] . [2015-09-26]. （原始内容存档于2014-07-14）.

[6] A.S. Yazdi, N. Razavi, S.R. Yazdinejad. Separation and determination of amitriptyline and nortriptyline by dispersive liquid–liquid microextraction combined with gas chromatography flame ionization detection. Talanta, 75 (2008), pp. 1293–1299

[AHFS2014-7] . The American Society of Health-System Pharmacists. [Sep 25, 2014]. （原始内容存档于2014-09-24）.

[8] Leucht, C; Huhn, M; Leucht, S. . The Cochrane Database of Systematic Reviews. December 2012, 12: CD009138. PMID 23235671. doi:10.1002/14651858.CD009138.pub2.

[Coch2015-9] Moore, RA; Derry, S; Aldington, D; Cole, P; Wiffen, PJ. . The Cochrane database of systematic reviews. 6 July 2015, 7: CD008242. PMID 26146793.

[10] . Australian Government. 3 March 2014 [22 April 2014]. （原始内容存档于2014-04-08）.

[11] . drugs.com. Sep 8, 2014 [25 September 2014]. （原始内容存档于2014-09-24）.

[12] Sneader, Walter. . Chichester: John Wiley & Sons. 2005: 414. ISBN 9780470015520.

[13] Fangmann P, Assion HJ, Juckel G, González CA, López-Muñoz F. . Journal of Clinical Psychopharmacology. February 2008, 28 (1): 1–4. PMID 18204333. doi:10.1097/jcp.0b013e3181627b60.

[14] (PDF). World Health Organization. October 2013 [22 April 2014]. （原始内容存档 (PDF)于2014-04-23）.

[15] . International Drug Price Indicator Guide. [2 December 2015]. （原始内容存档于2017年3月30日）.

[PDSP-17] Roth, BL; Driscol, J. . Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. 12 January 2011 [1 December 2013]. （原始内容存档于2013-11-08）.

[GG-18] Brunton, L; Chabner, B; Knollman, B. 12th. New York: McGraw-Hill Professional. 2010. ISBN 978-0-07-162442-8.