REVIEW Tianeptine was discovered by the French Society of Medical Research in the 1960s. It is used to treat major depressive episodes (mild, moderate, or severe). Tianeptine is a selective serotonin reuptake enhancer (SSRE), opposite to the action of SSRIs. Tianeptine enhances the extracellular concentration of dopamine in the nucleus accumbens and modulates the D2 and D3 dopamine receptors. There is also action on the NMDA and AMPA receptors. Recent reviews point to this pathway as a hypothesized mechanism of action, based on tianeptine's effect of reversing impaired neuroplasticity associated with stress. Tianeptine reduces the effects of serotonin in the limbic system and the pre-frontal cortex, giving rise to mood elevation. Like SSRIs, however, tianeptine's onset-of-action delay is approximately 2-6 weeks with improvements sometimes noticeable in as soon as one week, giving it a short-lived, but pleasant, stimulant effect experienced by some patients. Tianeptine has strong antidepressant and anxiolytic properties with a relative lack of sedative, anticholinergic and cardiovascular adverse effects, thus suggesting it is particularly suitable for use in elderly patients and in those following alcohol withdrawal; such patients can be more sensitive to the adverse effects of psychotropic drugs Recent interesting results indicate anticonvulsant and analgesic activity of tianeptine and its possible interaction with adenosine A1 receptors.
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