The pharmacokinetics of the antidepressant tianeptine and its main metabolite in healthy humans - influence of alcohol co-administration
by
Salvadori C, Ward C, Defrance R, Hopkins R.
Institut de Recherches Internationales Servier,
Neuilly-sur-Seine, France.
Fundam Clin Pharmacol. 1990;4(1):115-25.
ABSTRACTA balanced 3 way cross-over study involving 12 young healthy volunteers (6 men and 6 women) was used to determine the pharmacokinetic parameters of the antidepressant tianeptine following a single dose administered by oral and intravenous route. The influence of alcohol on the pharmacokinetics of tianeptine when given per os was also investigated. Kinetic parameters of metabolite MC5, the C5 side chain beta-oxidation product of tianeptine, were simultaneously determined. Following intravenous administration total clearance and volume of distribution of tianeptine were 230 +/- 59 ml.min-1 and 0.47 +/- 0.14 l.kg-1 respectively. When given orally, tianeptine was absorbed rapidly (tmax = 0.94 +/- 0.47 h). The mean systemic availability was estimated to be 99 +/- 29%. Tianeptine was eliminated from plasma with a half-life of 2.5 +/- 1.1 h, mainly via extrarenal route since its renal clearance averaged 0.38 +/- 0.47 ml.min-1. Plasma levels of metabolite MC5 were lower than those of the parent drug but decreased with a longer half-life (7.2 +/- 5.7 h). Alcohol co-administration decreased tianeptine absorption rate and lowered tianeptine plasma levels by about 30% but did not affect those of the MC5 metabolite.Cats
Alcoholics
Metabolism
Acute effects
Serotonin/forebrain
Tianeptine (Stablon)
Tianeptine: structure
Neurochemical profile
Alcohol: fatal combination
Tinaneptine v amitriptyline
Tianeptine for depressed alcoholics
Tianeptine for anxious depressives
Ultra-high dose psychostimulant effect
Tianeptine for anxiety induced by alcohol withdrawal
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