Tianeptine hepatotoxicity?

Hello r/noots,

I was wondering what everyone's thoughts were on the potential hepatotoxicity of tianeptine. I've recently been taking between 8-20mg on a daily basis and have noticed almost immediate beneficial results. However upon reading more about the compound I am weary about its reported hepatic side effects and DILI's. I am curious as to what you guys have to comment on regarding it's relative safety.

Posted Jan 14, 2016, 3:11 PM UTC

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micahjahnsNootropix•

I found a comment from u/MisterYouAreSoDumb on this subject that has a lot of good info on this subject:

"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.

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.

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.

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).

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."

So, the dose that you're taking is very well within the prescription guidelines. If you don't have any preexisting liver issues, I would say you don't really need to worry about liver issues with tianeptine.

4
HanflanderOP•

Thank you very much for the reply. I think I came across that post during my initial personal research. I also read the abstract of the case study in which the patient had what they concluded was an immunological response. A lot of research is behind paywalls so I get a bit worried in regards to information accessibility.

1