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THE GOOD DRUG GUIDEDepressive illness devastates millions of lives. Tianeptine (Stablon, Coaxil, Tatinol) is a neuroprotective antidepressant that reverses the neuronal damage and lasting misery caused by chronic, uncontrolled stress. Tianeptine acts both as a non-sedating anti-anxiety agent and a non-stimulating mood-brightener. Uniquely in clinical medicine, tianeptine acts as a selective serotonin reuptake enhancer. Its puzzling efficacy as an antidepressant illustrates how little modern psychiatric medicine really understands about mind, mood and depression.
However, a breakthrough in tianeptine research was announced in July 2014 with the unexpected discovery that tianeptine is a full agonist at the mu and delta opioid receptors with negligible effect at the kappa opioid receptors. Selective mu opioid agonists in the brain's "hedonic hotspots" typically induce euphoria. Selective kappa agonists typically induce dysphoria. The role of central delta opioid receptors is poorly understood. Dual activation of the mu and, less potently, delta opioid receptors may be critical to tianeptine's mood-brightening and anxiolytic effect - a therapeutic action seemingly unaccompanied by the physiological tolerance and dependence that have plagued traditional opioids. All previous research into tianeptine may need to be re-evaluated in this light. Neonatal Abstinence Syndrome following heavy use of tianeptine during pregnancy has been reported. The recently popular sulfate salt is less readily absorbed and excreted from the body than the sodium salt, allowing one-per-day dosing, smoother plasma concentrations, and minimal risk of abuse. More research is urgently needed.
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