阿米替林

**阿米替林**
临床资料
商品名（英语：Drug nomenclature）	Amitrip, Elevil, Endep, Levate
AHFS/Drugs.com	Monograph
MedlinePlus	a682388
核准状况	美 FDA: Amitriptyline;
怀孕分级	澳: C ; ;
给药途径	口服，肌注
ATC码	N06AA09 (WHO) ;
法律规范状态
法律规范	澳：限医生处方（S4）; 加：处方药（℞-only）; 英：处方药（℞-only） (POM); 美：处方药（℞-only）;
药物动力学数据
生物利用度	30–60%因经过首过代谢
血浆蛋白结合率	96%
药物代谢	肝脏 (CYP2D6)
生物半衰期	22.4 小时(26 hr for active metabolite, nortriptyline)
排泄途径	肾脏
识别信息
	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（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID7022594 ;
ECHA InfoCard	100.000.038
化学信息
化学式	C20H23N
摩尔质量	277.403 g/mol
3D模型（JSmol（英语：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（Amitriptyline）^[5]，商品名称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]。阿米替林也可以预防偏头痛、治疗包括纤维肌痛症及疱疹后神经痛（英语：postherpetic neuralgia）在内的神经性疼痛，偶尔也会被用于治疗失眠^[7]^[9]。该药属于口服药物^[7]。

常见的副作用包含口干、视觉障碍、姿位性低血压、嗜睡，以及便秘等等。严重的副作用可能会造成癫痫发作、尿滞留、青光眼，或是其他心脏问题，25岁以下的用药者甚至会有增加自杀念头的风险。该药切忌与单胺氧化酶抑制剂或希塞菩（英语：cisapride）等药物合用^[7]。妊娠时服用阿米替林可能具有风险^[10]^[7]，哺乳期间用药目前认为是安全的^[11]。该药为使用最广泛的一种三环类抗抑郁药（TCA），然其详细机转仍不清楚^[7]。

在1960年首次发现阿米替林^[12]，并于1961年被美国食品药品监督管理局核准^[13]。该药列名世界卫生组织基本药物标准清单当中，为基础医疗体系的必备用药之一^[14]。该药属于通用名药物^[7]，2014年每剂的批发价价格区间位于0.01至0.04美金之间^[15]，美国境内则约一剂0.20美金左右^[7]。

药理

药效

受体	K_i [nM]^[a] (阿米替林)^[16]^[17]	K_i [nM]^[b] (去甲替林)^[16]^[17]
SERT	3.13	16.5
NET	22.4	4.37
DAT	5380	3100
5-HT_1A（英语：5-HT1A receptor）	450	294
5-HT_1B（英语：5-HT1B receptor）	840	-
5-HT_2A（英语：5-HT2A receptor）	4.3	5
5-HT_2C（英语：5-HT2C receptor）	6.15	8.5
5-HT₆（英语：5-HT6 receptor）	103	148
5-HT₇（英语：5-HT7 receptor）	114	-
H₁（英语：Histamine H1 receptor）	1.1	15.1
H₃（英语：Histamine H3 receptor）	1000	-
H₄（英语：Histamine H4 receptor）	33.6	-
M₁（英语：Muscarinic acetylcholine receptor M1）	12.9	40
M₂（英语：Muscarinic acetylcholine receptor M2）	11.8	110
M₃（英语：Muscarinic acetylcholine receptor M3）	25.9	50
M₄（英语：Muscarinic acetylcholine receptor M4）	7.2	84
M₅（英语：Muscarinic acetylcholine receptor M5）	19.9	97
α₁（英语：alpha-1 adrenergic receptor）	24	55
α₂（英语：alpha-2 adrenergic receptor）	690	2030
D₁（英语：Dopamine D1 receptor）	89	-
D₂	1460	2570
D₃（英语：Dopamine D3 receptor）	206	-
D₅（英语：Dopamine D5 receptor）	170	-
σ（英语：Sigma receptor）	300	2000

备注

^ 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

^ ^1.0 ^1.1 ^1.2 ^1.3 AMITRIPTYLINE HYDROCHLORIDE tablet, film coated [Dispensing Solutions, Inc.]. DailyMed. Dispensing Solutions, Inc. September 2013 [1 December 2013]. （原始内容存档于2013-12-03）.
^ ^2.0 ^2.1 ^2.2 ^2.3 Levate (amitriptyline), dosing, indications, interactions, adverse effects, and more. Medscape Reference. WebMD. [1 December 2013]. （原始内容存档于2013-12-03）.
^ ^3.0 ^3.1 ^3.2 ^3.3 Endep Amitriptyline hydrochloride (PDF). TGA eBusiness Services. Alphapharm Pty Limited. 10 December 2012 [1 December 2013]. （原始内容存档于2017-08-13）.
^ ^4.0 ^4.1 ^4.2 ^4.3 Amitriptyline Tablets BP 50mg - Summary of Product Characteristics (SPC). electronic Medicines Compendium. Actavis UK Ltd. 24 March 2013 [1 December 2013]. （原始内容存档于2013-12-03）.
^ Oxford Dictionary: Definition of amitriptyline (British & World English). [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
^ ^7.0 ^7.1 ^7.2 ^7.3 ^7.4 ^7.5 ^7.6 ^7.7 ^7.8 Amitriptyline Hydrochloride. 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. Amitriptyline versus placebo for major depressive disorder.. 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. Amitriptyline for neuropathic pain in adults.. The Cochrane database of systematic reviews. 6 July 2015, 7: CD008242. PMID 26146793.
^ Prescribing medicines in pregnancy database. Australian Government. 3 March 2014 [22 April 2014]. （原始内容存档于2014-04-08）.
^ Amitriptyline Levels and Effects while Breastfeeding. drugs.com. Sep 8, 2014 [25 September 2014]. （原始内容存档于2014-09-24）.
^ Sneader, Walter. Drug Discovery a History.. Chichester: John Wiley & Sons. 2005: 414. ISBN 9780470015520.
^ Fangmann P, Assion HJ, Juckel G, González CA, López-Muñoz F. Half a century of antidepressant drugs: on the clinical introduction of monoamine oxidase inhibitors, tricyclics, and tetracyclics. Part II: tricyclics and tetracyclics. Journal of Clinical Psychopharmacology. February 2008, 28 (1): 1–4. PMID 18204333. doi:10.1097/jcp.0b013e3181627b60.
^ WHO Model List of Essential Medicines (PDF). World Health Organization. October 2013 [22 April 2014]. （原始内容存档 (PDF)于2014-04-23）.
^ Amitriptyline. International Drug Price Indicator Guide. [2 December 2015]. （原始内容存档于2017年3月30日）.
^ ^16.0 ^16.1 Roth, BL; Driscol, J. PDSP K_i Database. 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）.
^ ^17.0 ^17.1 Brunton, L; Chabner, B; Knollman, B. Goodman and Gilman's The Pharmacological Basis of Therapeutics 12th. New York: McGraw-Hill Professional. 2010. ISBN 978-0-07-162442-8.

[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] 1.0 ^1.1 ^1.2 ^1.3 AMITRIPTYLINE HYDROCHLORIDE tablet, film coated [Dispensing Solutions, Inc.]. DailyMed. Dispensing Solutions, Inc. September 2013 [1 December 2013]. （原始内容存档于2013-12-03）.

[MSR-2] 2.0 ^2.1 ^2.2 ^2.3 Levate (amitriptyline), dosing, indications, interactions, adverse effects, and more. Medscape Reference. WebMD. [1 December 2013]. （原始内容存档于2013-12-03）.

[TGA-3] 3.0 ^3.1 ^3.2 ^3.3 Endep Amitriptyline hydrochloride (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] 4.0 ^4.1 ^4.2 ^4.3 Amitriptyline Tablets BP 50mg - Summary of Product Characteristics (SPC). electronic Medicines Compendium. Actavis UK Ltd. 24 March 2013 [1 December 2013]. （原始内容存档于2013-12-03）.

[5] Oxford Dictionary: Definition of amitriptyline (British & World English). [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] 7.0 ^7.1 ^7.2 ^7.3 ^7.4 ^7.5 ^7.6 ^7.7 ^7.8 Amitriptyline Hydrochloride. 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. Amitriptyline versus placebo for major depressive disorder.. 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. Amitriptyline for neuropathic pain in adults.. The Cochrane database of systematic reviews. 6 July 2015, 7: CD008242. PMID 26146793.

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

[11] Amitriptyline Levels and Effects while Breastfeeding. drugs.com. Sep 8, 2014 [25 September 2014]. （原始内容存档于2014-09-24）.

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

[13] Fangmann P, Assion HJ, Juckel G, González CA, López-Muñoz F. Half a century of antidepressant drugs: on the clinical introduction of monoamine oxidase inhibitors, tricyclics, and tetracyclics. Part II: tricyclics and tetracyclics. Journal of Clinical Psychopharmacology. February 2008, 28 (1): 1–4. PMID 18204333. doi:10.1097/jcp.0b013e3181627b60.

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

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

[PDSP-17] 16.0 ^16.1 Roth, BL; Driscol, J. PDSP K_i Database. 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] 17.0 ^17.1 Brunton, L; Chabner, B; Knollman, B. Goodman and Gilman's The Pharmacological Basis of Therapeutics 12th. New York: McGraw-Hill Professional. 2010. ISBN 978-0-07-162442-8.

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