The metabolic pathways of tianeptine, a new antidepressant, in healthy volunteers.
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.
Grislain
L
L
Département de Métabolisme, Bio-Pharmacie Servier, Orléans, France.
Gele
P
P
Bertrand
M
M
Luijten
W
W
Bromet
N
N
Salvadori
C
C
Kamoun
A
A
D000928:Antidepressive Agents / Q000378:metabolism* / Q000493:pharmacokinetics; D000929:Antidepressive Agents, Tricyclic / Q000378:metabolism / Q000493:pharmacokinetics; D001711:Biotransformation; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D005243:Feces / Q000737:chemistry; D006207:Half-Life; D006801:Humans; D008297:Male; D013058:Mass Spectrometry; D012015:Reference Standards; D013841:Thiazepines / Q000378:metabolism* / Q000493:pharmacokinetics
D000928:Antidepressive Agents; D000929:Antidepressive Agents, Tricyclic; D013841:Thiazepines; C050504:tianeptine