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Fluoxetine kinetics and protein binding in normal and impaired renal function
Author(s) -
Aronoff George R,
Bergstrom Richard F,
Pottratz Scott T,
Sloan Rebecca S,
Wolen Robert L,
Lemberger Louis
Publication year - 1984
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1984.152
Subject(s) - fluoxetine , volume of distribution , metabolite , volunteer , chemistry , pharmacokinetics , pharmacology , active metabolite , urine , endocrinology , renal function , medicine , oral administration , hemodialysis , dialysis , biochemistry , biology , serotonin , receptor , agronomy
The effect of decreased renal function on the disposition and elimination of the nontricyclic antidepressant fluoxetine was examined in 25 adult male subjects after a single 40‐mg oral dose. Blood samples for the measurement of fluoxetine and its active metabolite norfluoxetine were drawn 13 times in the first 48 hr after dosing and thrice weekly thereafter for 4 wk. All urine was collected in daily aliquots for 4 wk and was assayed for fluoxetine and norfluoxetine concentrations. The extent of fluoxetine binding to plasma protein was determined by equilibrium dialysis. Kinetic analyses were by noncompartmental methods. The drug and its metabolite were distributed over a large apparent volume and both were eliminated slowly. No correlations between the degree of renal dysfunction and the rate of elimination, volume of distribution, or protein binding were found. Plasma concentrations of fluoxetine and norfluoxetine were not significantly changed by hemodialysis. Clinical Pharmacology and Therapeutics (1984) 36, 138–144; doi: 10.1038/clpt.1984.152