PMID: 2096105Jan 1, 1990Paper

Tianeptine and its main metabolite. Disposition in chronic renal failure and haemodialysis

Fundamental & Clinical Pharmacology
C SalvadoriD Friès

Abstract

The disposition of the antidepressant tianeptine and its MC5 metabolite (pentanoic acid analogue of tianeptine) was studied following a single 12.5 mg oral dose of tianeptine sodium salt in 20 patients with chronic renal failure. In 12 patients (group I) having a creatinine clearance of less than 19 ml.min-1 the pharmacokinetics parameters for tianeptine and MC5 metabolite were determined and compared with those obtained in a matched control group (group II). The other 8 patients (group III) were functionally anephric and were studied during 1 dialysis to assess the haemodialysis clearances of tianeptine and MC5 metabolite. The comparison between groups I and II showed that renal failure did not appear to affect the disposition of parent tianeptine. However, the MC5 metabolite terminal half-life was found to be increased in renal patients compared to controls (14.2 +/- 9.3 h vs 4.9 +/- 1.7 h). Due to a large interindividual variability the difference did not reach a significant level (P = 0.054). According to the antidepressant activity of the MC5 metabolite in pharmacological tests, the sustained rise in its plasma level suggests that a reduced daily dose should be administered and 12.5 mg of tianeptine should be given twice d...Continue Reading

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Citations

Jan 1, 1993·European Journal of Clinical Pharmacology·T H GraselaR Jochemsen
Aug 4, 2012·Nephrology, Dialysis, Transplantation : Official Publication of the European Dialysis and Transplant Association - European Renal Association·Evi V NaglerCarmine Zoccali
Apr 11, 2015·Seminars in Dialysis·Rachel F EylerAloun Mary Vilay
Jul 21, 2001·CNS Drugs·A J WagstaffC M Spencer
Mar 8, 2019·Revista brasileira de psiquiatria : orgão oficial da Associação Brasileira de Psiquiatria, Asociación Psiquiátrica de la América Latina·Juliana L Constantino, Vilma A Fonseca

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