Tianeptine (brand names Stablon, Coaxil, Tatinol, Tianeurax and Salymbra) is a drug used primarily in the treatment of major depressive disorder, although it may also be used to treat asthma or irritable bowel syndrome. Chemically it is a tricyclic antidepressant (TCA), but it has different pharmacological properties than typical TCAs as recent research suggests that tianeptine produces its antidepressant effects through indirect alteration of glutamate receptor activity (i.e., AMPA receptors and NMDA receptors) and release of BDNF, in turn affecting neural plasticity.
Tianeptine has antidepressant and anxiolytic (anti-anxiety) properties with a relative lack of sedative, anticholinergic and cardiovascular adverse effects, thus suggesting it is particularly suitable for use in the elderly and in those following alcohol withdrawal; such persons can be more sensitive to the adverse effects of psychotropic drugs. Recent results indicate possible anticonvulsant (anti-seizure) and analgesic (painkilling) activity of tianeptine via immediate or downstream modulation of adenosine A1 receptors (as the effects could be experimentally blocked by antagonists of this receptor).
Tianeptine is a low-affinity full agonist at the μ-opioid[note 1] and δ-opioid receptors with negligible effect at the κ-opioid receptors. μ-Opioid agonists typically induce euphoria, and in accordance, tianeptine does so at high doses well above the normal therapeutic range.
Tianeptine was discovered and patented by The French Society of Medical Research in the 1960s. Currently, tianeptine is approved in France and manufactured and marketed by Laboratories Servier SA; it is also marketed in a number of other European countries under the trade name “Coaxil” as well as in Asia (including Singapore) and Latin America as “Stablon” and “Tatinol” but it is not available in Australia, Canada, New Zealand, the U.K. or the U.S..