Comment · Sat, December 28, 2013 · Ceretropic
The antidepressants associated with greater risks of hepatotoxicity are ... , tianeptine, ... .
What they were answering
Direct reply to the original post in this thread.
u/MisterYouAreSoDumb · Ceretropic
Ohh that's nice, they did a Pubmed search for keywords regarding liver damage...
There is a low amount of renal metabolism with tianeptine, which can lead to reactive metabolites. However, the instances of this being a problem are very low.
http://www.sciencedirect.com/science/article/pii/0924933896823327
>Haematologic, and liver and renal function parameters were not
altered on tianeptine, and no signs of dependence were observed after
discontinuation of the treatment... The assessment of haematological, renal, metabolic and hepatic parameters confirmed the safety of tianeptine.
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http://link.springer.com/article/10.2165/00003088-198916030-00005
On the basis of this study, it appears unnecessary to modify the proposed dosage regimen used in clinical trials (tianeptine sodium salt 12.5mg 3 times daily) in chronic alcoholics with or without associated moderate cirrhosis.
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To be balanced, here is a case of a patient getting acute hepatitis with tianeptine. After discontinuing use, he showed complete recovery. They suggest it was an immuno-allergic reaction.
http://www.sciencedirect.com/science/article/pii/S0168827894802378
Hepatitis exhibited cholangitis-like clinical features and was associated with hypersensitivity manifestations suggestive of an immuno-allergic mechanism. Histological examination showed microvesicular steatosis. The discontinuation of tianeptine administration was followed by complete recovery.
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Here is a study that showed it can be metabolized into a reactive compound. It was not mediated by CYP2D6 or CYP1A1 enzymes, but rather by other CYP450 enzymes, and partially by glucocorticoidinducible isoenzymes.
http://www.sciencedirect.com/science/article/pii/000629529090554X
We conclude that tianeptine is activated by human liver cytochrome P450 into a reactive metabolite. This activation is mediated in part by glucocorticoidinducible isoenzymes but not by P450 IID6 (the isoenzyme which oxidizes debrisoquine) nor by P450 IA1 (an isoenzyme inducible by polycyclic aromatic compounds).
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Moral of the story, yes there is a small risk of liver issues with tianeptine use in some people. One should always be cognizant when using antidepressants, as they are not nootropics in the traditional sense.