Stablon Mechanism of Action

Pharmacotherapeutic group: Other Antidepressants. ATC code: N06AX14.
Pharmacology: Pharmacodynamics: Tianeptine is an antidepressant.
In animals, tianeptine has the following properties: tianeptine increases the spontaneous activity of pyramidal cells in the hippocampus and accelerates their recovery after functional inhibition; tianeptine increases the rate of serotonin re-uptake by neurons in the cortex and hippocampus.
In man, tianeptine is characterised by: marked action on somatic complaints, especially gastrointestinal complaints related to anxiety and mood disturbances.
Moreover, tianeptine has no effect on: sleep and alertness; the cholinergic system (no anticholinergic symptoms).
Pharmacokinetics: Gastrointestinal absorption is rapid and complete.
Distribution is rapid, and is associated with a high level of protein binding (approximately 94%).
The molecule is extensively metabolised in the liver by the processes of beta-oxidation and N-demethylation.
The elimination of tianeptine is characterised by a short terminal half-life of 2½ h and by essentially renal excretion of the metabolites.
In elderly subjects: pharmacokinetics studies performed in chronically treated elderly patients (aged over 70 years) demonstrated an increase of one hour in the elimination half-life.
In subjects with hepatic insufficiency: studies have shown that the effects of chronic alcoholism on the pharmacokinetic parameters are negligible, even when the alcoholism is associated with cirrhosis of the liver.
In subjects with renal insufficiency: studies have shown an increase of one hour in the elimination half-life.
Toxicology: Preclinical safety data: A study demonstrated in rats a decrease in reproductive performance in females (increase in pre-implantation losses) at a maternotoxic dose of 45 mg/kg/day.