Abstract
The pharmacokinetics of the 5-HT3 receptor antagonist ondansetron following an 8 mg i.v. dose were investigated in 12 subjects previously phenotyped with debrisoquine. Six subjects were poor metabolisers (debrisoquine metabolic ratios 29-131) and six were extensive metabolisers (debrisoquine metabolic ratios 0.45-3.4). There was no significant difference in AUC, Cmax, CL or t1/2 between the poor and extensive metabolisers. It is concluded that ondansetron clearance is not mediated exclusively by cytochrome P-450 2D6.
MeSH terms
-
Adult
-
Chromatography, High Pressure Liquid
-
Cytochrome P-450 CYP2D6
-
Cytochrome P-450 Enzyme System / genetics
-
Cytochrome P-450 Enzyme System / metabolism
-
Debrisoquin / metabolism*
-
Female
-
Half-Life
-
Humans
-
Infusions, Intravenous
-
Male
-
Metabolic Clearance Rate
-
Mixed Function Oxygenases / genetics
-
Mixed Function Oxygenases / metabolism
-
Ondansetron / administration & dosage
-
Ondansetron / blood
-
Ondansetron / pharmacokinetics*
-
Phenotype
Substances
-
Ondansetron
-
Cytochrome P-450 Enzyme System
-
Mixed Function Oxygenases
-
Cytochrome P-450 CYP2D6
-
Debrisoquin