The pharmacokinetics of ondansetron after intravenous injection in healthy volunteers phenotyped as poor or extensive metabolisers of debrisoquine.
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.
Department of Clinical Pharmacokinetics, Glaxo Group Research Ltd, Greenford, Middlesex.
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Palmer
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D000328:Adult; D002851:Chromatography, High Pressure Liquid; D019389:Cytochrome P-450 CYP2D6; D003577:Cytochrome P-450 Enzyme System / Q000235:genetics / Q000378:metabolism; D003647:Debrisoquin / Q000378:metabolism*; D005260:Female; D006207:Half-Life; D006801:Humans; D007262:Infusions, Intravenous; D008297:Male; D008657:Metabolic Clearance Rate; D006899:Mixed Function Oxygenases / Q000235:genetics / Q000378:metabolism; D017294:Ondansetron / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D010641:Phenotype
D017294:Ondansetron; D003577:Cytochrome P-450 Enzyme System; D006899:Mixed Function Oxygenases; D019389:Cytochrome P-450 CYP2D6; D003647:Debrisoquin