Tianeptine shows efficacy against serious depressive episodes (major depression), comparable to amitriptyline, imipramine and fluoxetine, but with significantly fewer side effects.

The risk or severity of adverse effects can be increased when Alverine is combined with Tianeptine. The risk or severity of serotonin syndrome can be increased when Amantadine is combined with Tianeptine.

Tianeptine is an antidepressant agent with a novel neurochemical profile. It increases serotonin (5-hydroxytryptamine; 5-HT) uptake in the brain (in contrast with most antidepressant agents) and reduces stress-induced atrophy of neuronal dendrites.

Supposedly, Tianeptine, in contrast to other anti-depressants, stimulates release of neurotransmitter dopamine in nucleus Accumbens, that probably determine addictive potential of this drug.

At large doses, tianeptine is known to produce opioid-like recreational effects, such as stimulation and sedation, motivation, and euphoria.

At a standard dose, people who take tianeptine don’t get a high, build up tolerance, or have withdrawal symptoms if they stop. Tianeptine hasn’t been considered for approval as an antidepressant in the United States because it’s a generic and therefore not a promising money-maker.

This antidepressant agent neither inhibited paradoxical sleep nor increased slow wave sleep. However, tianeptine induced a slight, but significant increase in wakefulness during the first hour following its administration, and had no sedative effects.

Tianeptine at high doses can be dangerous and can cause an overdose. A 2018 study reports 15 cases of tianeptine overdose, about half being in combination with another substance, 3 of which resulted in death.

Selling it as a supplement is illegal, but tianeptine is widely available online even now. Numerous studies have found tianeptine is a hazard to public health and may be a risk for abuse, overdose and addiction. Yet the U.S. Food and Drug Administration has only recently taken any action against sellers.

It has been found to act as an atypical agonist of the μ-opioid receptor with clinically negligible effects on the δ- and κ-opioid receptors. Tianeptine was discovered and patented by the French Society of Medical Research in the 1960s.

In terms of chemical structure, it is similar to tricyclic antidepressants (TCAs), but it has significantly different pharmacology and important structural differences, so it is not usually grouped with them.

Tianeptine can also cause severe withdrawal symptoms after prolonged use at high doses which should prompt extreme caution. (nM), unless otherwise noted. The smaller the value, the more strongly the drug interacts with the site.

Research indicates possible anticonvulsant (anti-seizure) and analgesic (painkilling) activity of tianeptine via downstream modulation of adenosine A 1 receptors (as the effects could be experimentally blocked by antagonists of this receptor). The bioavailability of tianeptine is approximately 99%. Its plasma protein binding is about 95%.