title: Pharmacokinetic and metabolic parameters of tianeptine in healthy volunteers and in populations with risk factors.
abstract: Following oral administration in the fasting healthy subject, the mean maximum concentration of tianeptine is 334 +/- 79 ng/ml. Absorption of tianeptine from the tablet form is rapid and complete. Maximum plasma concentration is obtained by the first hour following administration (0.94 +/- 0.47 h). Absolute bioavailability is 99 +/- 29%. Tianeptine is thus rapidly and completely absorbed in the tablet form and is not subject to first-pass effect. Distribution of tianeptine in the body is characterized by the following: its rapidity, the mean distribution half-life being about 0.7 h; its limited extent, the apparent volume of distribution being about 0.8 L/kg (0.77 +/- 0.31 L/kg); and protein binding, which averages 93.8 +/- 2.4%. Elimination of tianeptine is characterized by a short mean half-life of 2 h 30 min (2.5 +/- 1.1 h) and by renal excretion of 0.4 ml/min (0.4 +/- 0.4 ml/min). Tianeptine is extensively metabolized. Major metabolites are analogs of tianeptine with a C5 and C3 lateral chain and a N-demethylated derivative. Studies have shown negligible influence on pharmacokinetic parameters of chronic alcoholism even in case of hepatic cirrhosis. In renal failure, and in the elderly, studies have revealed a 1-h prolongation of elimination half-life which suggests that the dosage should be limited to two tablets per day in such cases.
authors.affiliation: Hôpital Central, Nancy, France.
authors.forename: R J
authors.initials: RJ
authors.lastname: Royer
authors.forename: H
authors.initials: H
authors.lastname: Albin
authors.forename: D
authors.initials: D
authors.lastname: Barrucand
authors.forename: C
authors.initials: C
authors.lastname: Salvadori-Failler
authors.forename: A
authors.initials: A
authors.lastname: Kamoun
mesh_terms: D000284:Administration, Oral; D000929:Antidepressive Agents, Tricyclic / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D001682:Biological Availability; D006207:Half-Life; D006801:Humans; D012307:Risk Factors; D013607:Tablets; D013841:Thiazepines / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*
chemical_list: D000929:Antidepressive Agents, Tricyclic; D013607:Tablets; D013841:Thiazepines; C050504:tianeptine