Table 1.
In vivo low dose drug cocktail phenotyping for assessment of drug-metabolizing cytochrome P450 (CYP) enzymes including selective substrates employed, respective doses and phenotyping parameters.
Drug-metabolizing CYP enzymes | Drug | Dose (mg) | Phenotyping parameter (unit) |
---|---|---|---|
CYP1A2 | Caffeine | 150 | Oral caffeine clearance (ml/min per kg body weight) |
CYP2C9 | Tolbutamide | 125 | Plasma concentration of tolbutamide 24 h post dose (μg/ml) |
CYP2C19 | Omeprazole | 20 | Ratio of the molar plasma concentrations of omeprazole over 5-hydroxyomeprazole 3 h post dose (−) |
CYP2D6 | Dextromethorphan hydrobromide | 30 | Ratio of the molar plasma concentrations of dextromethorphan over dextrorphan 3 h post dose (−) |
CYP3A4 | Midazolam | 2 | Oral midazolam clearance (L/hl) |