The metabolic pathways of tianeptine, a new
antidepressant, in healthy volunteers
Grislain L, Gele P, Bertrand M, Luijten W,
Bromet N, Salvadori C, Kamoun A.
Departement de Metabolisme,
Bio-Pharmacie Servier, Orleans, France.
Drug Metab Dispos. 1990 Sep-Oct;18(5):804-8.
ABSTRACTThe metabolism of tianeptine, a novel antidepressant that presents original neurochemical properties, was studied after a single oral administration of radioisotopically (14C) labeled compound to six healthy male volunteers. After 7 days, approximately 66% of the dose was eliminated by renal excretion (55% during the first 24 hr). Tianeptine is extensively metabolized, and 24 hr after the administration, the unchanged molecule contributed in urine for less than 3% of the administered dose. Chromatographic and mass spectral studies showed that beta-oxidation of the amino acid side chain is the major route of biotransformation for tianeptine. Three major metabolites, accounting for 29% of the dose, were products of beta-oxidation. The metabolite profiles of tianeptine in feces and plasma were qualitatively similar to that in urine.Metabolism
Tianeptine for anxious depressives
Tianeptine-induced serotonin uptake increase
Place of tianeptine (Stablon) among antidepressants
Structure-activity relationships/tricyclic antidepressants
and further reading
The Abolitionist Project
The Hedonistic Imperative
The Reproductive Revolution
Critique of Huxley's Brave New World
The Good Drug Guide
The Responsible Parent's Guide
To Healthy Mood Boosters For All The Family