噻奈普汀
外观
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臨床資料 | |
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商品名 | Stablon, 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 | |
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 | |
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CAS号 | 72797-41-2 ![]() 30123-17-2(钠盐) 1224690-84-9(硫酸盐) |
PubChem CID | |
IUPHAR/BPS | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.069.844、100.131.750 |
化学信息 | |
化学式 | C21H25ClN2O4S |
摩尔质量 | 436.95 g·mol−1 |
3D模型(JSmol) | |
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噻奈普汀是一种非典型抗抑郁药,主要用于重性抑郁疾患的治疗,也可以用来治疗焦虑、气喘和大肠激躁症。[1][2][3]
噻奈普汀具有抗抑郁和抗焦虑作用,[9]且镇静性、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-阿片受体的非典型激动剂,而对δ-阿片受体和κ-阿片受体的影响可忽略不计。[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 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、英国或美国销售。[14][15]
由于其μ-阿片受体激动剂效应,远高于治疗剂量的噻奈普汀可以造成类似阿片类药物的欣快感。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
[编辑]- ^ 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).
- ^ 2.0 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).
- ^ 3.0 3.1 Tianeptine. [2022-03-03]. (原始内容存档于2012-01-25).
- ^ Tianeptine – AdisInsight. AdisInsight. Springer. [31 January 2016]. (原始内容存档于2022-03-03).
- ^ 存档副本. [2022-03-03]. (原始内容存档于2020-12-13).
- ^ 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.
- ^ 7.0 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.
- ^ 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.
- ^ 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).
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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).
- ^ Tianeptine Sodium. Martindale: The Complete Drug Reference (London, UK: Pharmaceutical Press). 5 December 2011 [2 December 2013].
- ^ 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.
- ^ 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).
- ^ 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).
- ^ 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).
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