噻奈普汀

噻奈普汀是一种非典型抗抑郁药英语atypical antidepressant,主要用于重性抑郁疾患的治疗,也可以用来治疗焦虑气喘大肠激躁症[1][2][3]

噻奈普汀
臨床資料
商品名英语Drug nomenclatureStablon, Coaxil, others
其他名稱S-1574;[1][2][3] JNJ-39823277; TPI-1062[4]
AHFS/Drugs.com国际药品名称
给药途径口服
ATC碼
法律規範狀態
法律規範
  • In general: Rx-only
    US: not FDA approved, schedule 1 in MN, schedule 2 in OK, MI & AL
    AU: S4[5]
    Others: controlled in FR, BH, SG)
藥物動力學數據
生物利用度99%[6][7]
血漿蛋白結合率95%[7]
药物代谢Hepatic[7]
生物半衰期2.5–3 hours[6][7]
4–9 hours (elderly)[7][8]
排泄途徑尿:65%[6]
大便:15%[7]
识别信息
  • 7-[(3-Chloro-6-methyl-5,5-dioxo-11H-benzo[c][2,1]benzothiazepin-11-yl)amino]heptanoic acid
CAS号72797-41-2  checkY
30123-17-2盐)
1224690-84-9硫酸盐
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.069.844、​100.131.750 編輯維基數據鏈接
化学信息
化学式C21H25ClN2O4S
摩尔质量436.95 g·mol−1
3D模型(JSmol英语JSmol
  • Clc1cc2c(cc1)C(c3c(N(C)S2(=O)=O)cccc3)NCCCCCCC(=O)O
  • InChI=1S/C21H24ClN2NaO4S/c1-24-18-9-6-5-8-16(18)21(23-13-7-3-2-4-10-20(25)26)17-12-11-15(22)14-19(17)29(24,27)28/h5-6,8-9,11-12,14,21,23H,2-4,7,10,13H2,1H3,(H,25,26) checkY
  • Key:JICJBGPOMZQUBB-UHFFFAOYSA-N checkY

噻奈普汀具有抗抑郁和抗焦虑作用,[9]镇静性、抗胆碱剂作用和心血管副作用相对较少。[7][10]人们已发现它是μ-阿片受体英语μ-opioid receptor的非典型激动剂,而对δ-阿片受体英语δ-opioid receptorκ-阿片受体英语κ-opioid receptor的影响可忽略不计。[11][12][13]

噻奈普汀由法国医学研究学会于1960年代发现并获得专利。今天,噻奈普汀在法国获得批准,由Laboratoires Servier英语Laboratoires Servier SA生产和销售。它还在许多其它欧洲国家以商品名Coaxil,以及在亚洲(包括新加坡)和拉丁美洲以商品名Stablon和Tatinol销售,但噻奈普汀不在澳大利亚加拿大新西兰英国美国销售。[14][15]

由于其μ-阿片受体英语μ-opioid receptor激动剂效应,远高于治疗剂量的噻奈普汀可以造成类似阿片类药物欣快感。在这种用法下,噻奈普汀可以成瘾,并且药物戒断反应严重。[16][17]由于滥用泛滥,新加坡、俄罗斯已加紧对此药物的管制。[18][19]

参考资料

  1. ^ 1.0 1.1 Elks J. The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. 14 November 2014: 1195– [2022-03-03]. ISBN 978-1-4757-2085-3. (原始内容存档于2020-08-31). 
  2. ^ 2.0 2.1 Index Nominum 2000: International Drug Directory. Taylor & Francis. 2000: 1024– [2022-03-03]. ISBN 978-3-88763-075-1. (原始内容存档于2020-09-07). 
  3. ^ 3.0 3.1 Tianeptine. [2022-03-03]. (原始内容存档于2012-01-25). 
  4. ^ Tianeptine – AdisInsight. AdisInsight. Springer. [31 January 2016]. (原始内容存档于2022-03-03). 
  5. ^ 存档副本. [2022-03-03]. (原始内容存档于2020-12-13). 
  6. ^ 6.0 6.1 6.2 Royer RJ, Albin H, Barrucand D, Salvadori-Failler C, Kamoun A. Pharmacokinetic and metabolic parameters of tianeptine in healthy volunteers and in populations with risk factors. Clinical Neuropharmacology. 1988, 11 (Suppl 2): S90–6. PMID 3180120. 
  7. ^ 7.0 7.1 7.2 7.3 7.4 7.5 7.6 Wagstaff AJ, Ormrod D, Spencer CM. Tianeptine: a review of its use in depressive disorders. CNS Drugs. March 2001, 15 (3): 231–59. PMID 11463130. doi:10.2165/00023210-200115030-00006. 
  8. ^ Carlhant D, Le Garrec J, Guedes Y, Salvadori C, Mottier D, Riche C. Pharmacokinetics and bioavailability of tianeptine in the elderly. Drug Investigation. September 1990, 2 (3): 167–172. S2CID 56502717. doi:10.1007/BF03259191. 
  9. ^ Defrance R, Marey C, Kamoun A. Antidepressant and anxiolytic activities of tianeptine: an overview of clinical trials (PDF). Clinical Neuropharmacology. 1988, 11 (Suppl 2): S74–82. PMID 2902922. (原始内容 (PDF)存档于4 April 2016). 
  10. ^ Kasper S, McEwen BS. Neurobiological and clinical effects of the antidepressant tianeptine. CNS Drugs. 2008, 22 (1): 15–26. PMID 18072812. S2CID 30330824. doi:10.2165/00023210-200822010-00002. 
  11. ^ Gassaway MM, Rives ML, Kruegel AC, Javitch JA, Sames D. The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist. Translational Psychiatry. July 2014, 4 (7): e411. PMC 4119213 . PMID 25026323. doi:10.1038/tp.2014.30. 
  12. ^ Berridge KC, Kringelbach ML. Affective neuroscience of pleasure: reward in humans and animals. Psychopharmacology. August 2008, 199 (3): 457–80. PMC 3004012 . PMID 18311558. doi:10.1007/s00213-008-1099-6. 
  13. ^ El Zahran T, Schier J, Glidden E, Kieszak S, Law R, Bottei E, et al. Characteristics of Tianeptine Exposures Reported to the National Poison Data System - United States, 2000-2017. MMWR. Morbidity and Mortality Weekly Report. August 2018, 67 (30): 815–818. PMC 6072055 . PMID 30070980. doi:10.15585/mmwr.mm6730a2. 
  14. ^ Akiki T. The etiology of depression and the therapeutic implications. Glob. J. Med. Res. [2022-03-03]. ISSN 2249-4618. (原始内容存档于2016-11-03). 
  15. ^ Tianeptine Sodium. Martindale: The Complete Drug Reference (London, UK: Pharmaceutical Press). 5 December 2011 [2 December 2013]. 
  16. ^ Lauhan R, Hsu A, Alam A, Beizai K. Tianeptine Abuse and Dependence: Case Report and Literature Review. Psychosomatics. November 2018, 59 (6): 547–553. PMID 30149933. S2CID 52099752. doi:10.1016/j.psym.2018.07.006. 
  17. ^ Vadachkoria D, Gabunia L, Gambashidze K, Pkhaladze N, Kuridze N. Addictive potential of Tianeptine - the threatening reality. Georgian Medical News. September 2009, (174): 92–4 [2024-07-19]. PMID 19801742. (原始内容存档于2023-12-09). 
  18. ^ World Health Organization. Pharmaceuticals: Restrictions in use and availability, March 2001 (PDF). 2001 [24 July 2008]. (原始内容 (PDF)存档于17 November 2008). 
  19. ^ Ives R. Assessment Mission Report for the SCAD V Programme, Component on Prevention and on Media Work (PDF). 2008 [4 November 2008]. (原始内容 (PDF)存档于1 December 2010).