The metabolic pathways of tianeptine, a new
antidepressant, in healthy volunteers

by
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.


ABSTRACT

The 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
MC5 metabolite
Tianeptine: profile
Serotonin/forebrain
Tianeptine (Stablon)
Tianeptine: structure
Melancholic depression
Microvesicular steatosis
Tianeptine for anxious depressives
Tianeptine-induced serotonin uptake increase
Place of tianeptine (Stablon) among antidepressants
Structure-activity relationships/tricyclic antidepressants


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