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噻奈普汀

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噻奈普汀
臨床資料
商品名英語Drug nomenclatureStablon, Coaxil, others
其他名稱S-1574;[1][2][3] JNJ-39823277; TPI-1062[4]
AHFS/Drugs.com國際藥品名稱
給藥途徑口服
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]
藥物代謝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]
識別資訊
  • 7-[(3-Chloro-6-methyl-5,5-dioxo-11H-benzo[c][2,1]benzothiazepin-11-yl)amino]heptanoic acid
CAS號72797-41-2  checkY
30123-17-2鹽)
1224690-84-9硫酸鹽
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英語CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.069.844、​100.131.750 編輯維基數據鏈接
化學資訊
化學式C21H25ClN2O4S
摩爾質量436.95 g·mol−1
3D模型(JSmol英語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

噻奈普汀是一種非典型抗抑鬱藥英語atypical antidepressant,主要用於重性抑鬱疾患的治療,也可以用來治療焦慮氣喘大腸激躁症[1][2][3]

噻奈普汀具有抗抑鬱和抗焦慮作用,[9]鎮靜性、抗膽鹼劑作用和心血管副作用相對較少。[7][10]人們已發現它是μ-阿片受體英語μ-opioid receptor的非典型激動劑,而對δ-阿片受體英語δ-opioid receptorκ-阿片受體英語κ-opioid receptor的影響可忽略不計。[11][12][13]

噻奈普汀由法國醫學研究學會於1960年代發現並獲得專利。今天,噻奈普汀在法國獲得批准,由Laboratoires Servier英語Laboratoires Servier SA生產和銷售。它還在許多其它歐洲國家以商品名Coaxil,以及在亞洲(包括新加坡)和拉丁美洲以商品名Stablon和Tatinol銷售,但噻奈普汀不在澳大利亞加拿大新西蘭英國美國銷售。[14][15]

由於其μ-阿片受體英語μ-opioid receptor激動劑效應,遠高於治療劑量的噻奈普汀可以造成類似阿片類藥物欣快感。在這種用法下,噻奈普汀可以成癮,並且藥物戒斷反應嚴重。[16][17]由於濫用泛濫,新加坡、俄羅斯已加緊對此藥物的管制。[18][19]

參考資料

[編輯]
  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. (原始內容存檔於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. (原始內容存檔於2020-09-07). 
  3. ^ 3.0 3.1 Tianeptine. [2022-03-03]. (原始內容存檔於2012-01-25). 
  4. ^ Tianeptine – AdisInsight. AdisInsight. Springer. [31 January 2016]. (原始內容存檔於2022-03-03). 
  5. ^ 存档副本. [2022-03-03]. (原始內容存檔於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. (原始內容 (PDF)存檔於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可免費查閱. 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可免費查閱. 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可免費查閱. 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. (原始內容存檔於2016-11-03). 
  15. ^ Tianeptine Sodium. Martindale: The Complete Drug Reference (London, UK: Pharmaceutical Press). 5 December 2011 [2 December 2013]. 
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  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. (原始內容存檔於2023-12-09). 
  18. ^ World Health Organization. Pharmaceuticals: Restrictions in use and availability, March 2001 (PDF). 2001 [24 July 2008]. (原始內容 (PDF)存檔於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]. (原始內容 (PDF)存檔於1 December 2010).