阿米替林

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阿米替林
Amitriptyline2DACS.svg
Amitriptyline-from-picrate-xtal-3D-balls.png
系统(IUPAC)命名名称
3-(10,11-Dihydro-5H-dibenzo[a,d]cycloheptene-5-ylidene)-N,N-dimethylpropan-1-amine
临床数据
商品名 Amitrip, Elevil, Endep, Levate
Drugs.com Monograph
MedlinePlus a682388
医疗法规
妊娠分级
  • AU: C
  • US: C (不排除有风险的可能)
给药途径 口服,肌注
合法狀態
合法状态
药代动力学数据
生物利用度 30–60%因经过首过代谢
蛋白结合度 96%[1][2][3][4]
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 肾脏[1][2][3][4]
识别信息
CAS注册号 50-48-6 ✓
549-18-8 (hydrochloride)
ATC代码 N06AA09
PubChem CID 2160
IUPHAR/BPS英语IUPHAR/BPS 200
DrugBank DB00321 ✓
ChemSpider 2075 ✓
UNII 1806D8D52K ✓
KEGG D07448 ✓
ChEBI CHEBI:2666 ✓
ChEMBL英语ChEMBL CHEMBL629 ✓
化学信息
化学式 C20H23N
摩尔质量 277.403 g/mol
  (verify)

阿米替林Amitriptyline[5],商品名稱Elavil,是使用最广泛的一种三环类抗抑郁药[6] 阿米替林可以治疗许多精神障碍[7],包括重度抑郁症焦虑症,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疱疹後神經痛英语postherpetic neuralgia在内的神經病變痛英语neuropathic pain,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希塞菩英语cisapride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]

作用机制[编辑]

受体 Ki [nM][a]
(阿米替林)[16][17]
Ki [nM][b]
(去甲替林)[16][17]
SERT 3.13 16.5
NET 22.4 4.37
DAT 5380 3100
5-HT1A英语5-HT1A receptor 450 294
5-HT1B英语5-HT1B receptor 840 -
5-HT2A英语5-HT2A receptor 4.3 5
5-HT2C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

備註[编辑]

  1. ^ These Ki values are averaged binding affinities towards cloned human receptors when available.
  2. ^ As with amitriptyline, these Kivalues are averaged binding affinities towards cloned human receptors when available.

引用[编辑]

  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]. 
  2. ^ 2.0 2.1 2.2 2.3 Levate (amitriptyline), dosing, indications, interactions, adverse effects, and more. Medscape Reference. WebMD. [1 December 2013]. 
  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]. 
  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]. 
  5. ^ Oxford Dictionary: Definition of amitriptyline (British & World English)
  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
  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]. 
  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. 
  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]. 
  11. ^ Amitriptyline Levels and Effects while Breastfeeding. drugs.com. Sep 8, 2014 [25 September 2014]. 
  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]. 
  15. ^ Amitriptyline. International Drug Price Indicator Guide. [2 December 2015]. 
  16. ^ 16.0 16.1 Roth, BL; Driscol, J. PDSP Ki 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]. 
  17. ^ 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.