Okay, so, there’s a new drug that being sold at smoke shops and gas stations here in the states called tianeptine. I personally know a family run shop that get’s it formulated with kava extract from a lab over in Denver. I have yet to try this product, but am intrigued, upon doing research. The purpose of the following is to give a little backstory on the pharmacology and history of this medication.
Disclaimer:This article is not medical advice. I am not encouraging recreational use of any substance. The outcomes of any choice the reader makes with the following info is solely the reader’s responsibility. Always seek medical guidance from a licensed physician.
Tianeptine was discovered and patented by the French Society of Medical Research in the sixties. It’s currently approved by France’s FDA. It is manufactured by Servier Laboratories and sold under the name Coaxil in a number of European countries . It’s also used in parts of Asia and Latin America under the names Stablon and Tatinol [1].
From my research, it’s primarily prescribed for depressive episodes as seen in Major Depressive Disorder [2]. Many antidepressant (SSRIs and SNRIs) take 4-8 weeks to fully take effect [3], which makes quicker acting medications better for episodic disorders. Tianeptine is also extremely anxiolytic, and has has been used to treat a spectrum of anxiety disorders. A 2004 study showed it to be equivalent to paroxetine in panic blocking effects [4]. This would make it would seem to be especially useful to those with comorbid anxiety and depression [5].
Pharmacologically tianeptine is multifaceted.
It is a full mu opioid receptor agonist as well a full delta opioid receptor agonist, albeit at a much lower potency [6]. A 2017 study on rats exploring this mechanism showed that the rats didn’t develop tolerance or withdrawal [7], yet this is heavily contradicted by anecdotal reports here in the states.
In contrast to typical antidepressants, tianeptine increases serotonin re-uptake in humans [5]. I have yet to see a study that concludes through what mechanism this occurs, though wikipedia has it listed as tianeptine’s interaction with SERT. There is one article I found that states it is likely not due to SERT.
Tianeptine also has action on and inhibition of Glutamate receptors. This allows it to be neuroprotective in times of stress and reverse stress induced structural and cellular changes. Although this mechanism of action is a little over my head, it is suspected to be a promising way of treating depression [8].
It is not subject to first-pass hepatic metabolism and has high bioavailability.
[1] https://www.drugs.com/international/tianeptine.html
[2] https://go.drugbank.com/articles/A31969
[4]https://pubmed.ncbi.nlm.nih.gov/15582922/
[5]https://pubmed.ncbi.nlm.nih.gov/11463130/
[6]https://pubmed.ncbi.nlm.nih.gov/25026323/
[7]https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5561344/
[8] https://pubmed.ncbi.nlm.nih.gov/18072812/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5561344/
Leave a Reply