Pharmacokinetics of the antidepressant tianeptine
at steady state in the elderly

by
Demotes-Mainard F, Galley P, Manciet G,
Vinson G, Salvadori C.
Centre de Pharmacologie Clinique,
Universite de Bordeaux II, France.
J Clin Pharmacol. 1991 Feb;31(2):174-8.


ABSTRACT

The pharmacokinetics of tianeptine, an antidepressant with an original serotoninergic neurochemical action, was investigated in elderly patients. Kinetic profiles were developed in 12 elderly patients (age range: 72-81 yr) after single (12.5 mg) dose and multiple oral dosages (12.5 mg tid for 17 days). Multiple dosing of tianeptine was well tolerated; no accumulation of the unchanged drug was observed. Tianeptine and its MC5 metabolite (C5 acid analogue of tianeptine) reached maximum plasma levels after 1.81 +/- .99 and 2.96 +/- 1.44 hr, respectively, with values of 353 +/- 198 and 81 +/- 20 ng/mL, respectively, after a single dose and of 405 +/- 202 and 175 +/- 85 ng/mL, respectively, after multiple dosing. Minimum plasma concentrations of tianeptine were about half those of its MC5 metabolite (68 +/- 41 and 121 +/- 64 ng/mL-1 on day 5), and for each compound, they were not statistically different from day 5 to day 18 of the chronic administration. This finding is compatible with the terminal half-lives that were observed after the single dose that was 2.8 +/- .9 hr for tianeptine and 12.3 +/- 7 hr for the MC5 metabolite. For both compounds, the area-under-the-plasma levels time curve at steady state was as predicted from the initial single dose that showed no deviation from linearity with time. The kinetics of tianeptine in elderly patients were similar to those reported for young adults. However, MC5 metabolite plasma levels were higher in elderly patients than in younger patients.
Elderly depression
Tianeptine (Stablon)
Tianeptine: structure
Melancholic depression
Tianeptine for anxious depressives
A population pharmacokinetic database
Electrophysiological effects of tianeptine
Treatment of depressed elderly with tianeptine


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