PHARMACOKINETICS OF FLUOXETINE AND NORFLUOXETINE AFTER ADMINISTRATION OF SINGLE ORAL DOSE OF FLUOXETINE TO HEALTHY VOLUNTEERS.
LAURIAN VLASE, SORIN E. LEUCUŢA
University of Medicine and Pharmacy “Iuliu Hatieganu”, Faculty of Pharmacy, Department of Pharmaceutical Technology and Biopharmaceutics, 13 Emil Isac, 400023, Cluj, Cluj-Napoca, Romania vlaselaur@yahoo.com

Abstract:

A pharmacokinetic study of fluoxetine after administration of a single oral dose of 40 mg fluoxetine to 18 healthy volunteers was realized. Twelve pharmacokinetic models and compartmental analysis were used in order to calculate the pharmacokinetic parameters for fluoxetine and its metabolite. The representative model involves a 0 order absorption kinetic for fluoxetine and first pass hepatic effect, bicompartmental distribution and a 1st order elimination kinetics. The appearance of norfluoxetine is due to both presystemic and systemic metabolism of fluoxetine and is characterized by monocompartmental distribution and a 1st order elimination kinetic. Using the representative model for fluoxetine and norfluoxetine there was calculated the following pharmacokinetic parameters: the volume of distribution, the absorption time, the first-pass effect and the rate constants of distribution, metabolisation and non-metabolic elimination.

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