Inhibitor (μM) | Mean (± S.E.) Fraction (Rv) of Control (Uninhibited) Diazepam 3-Hydroxylation Velocity at Protein Concentration | Free IC501-150 | |||||||
---|---|---|---|---|---|---|---|---|---|
0.0625 | 0.125 | 0.25 | 0.5 | 0.75 | 1.0 | 2.0 | 3.0 | ||
mg/ml | μM | ||||||||
Ritonavir (0.05) | 0.21 ± 0.09 | 0.27 ± 0.12 | 0.45 ± 0.11 | 0.61 ± 0.13 | 0.67 ± 0.09 | 0.72 ± 0.08 | 0.86 ± 0.05 | 0.92 ± 0.04 | 0.0035 ± 0.0016 |
Ketoconazole (0.05) | 0.24 ± 0.04 | 0.21 ± 0.05 | 0.44 ± 0.14 | 0.53 ± 0.11 | 0.61 ± 0.09 | 0.70 ± 0.08 | 0.83 ± 0.06 | 0.89 ± 0.03 | 0.0059 ± 0.0028 |
OH-Itraconazole (0.25) | 0.32 ± 0.05 | 0.37 ± 0.10 | 0.37 ± 0.06 | 0.45 ± 0.06 | 0.55 ± 0.04 | 0.59 ± 0.06 | 0.76 ± 0.07 | 0.79 ± 0.05 | 0.095 ± 0.01 |
Itraconazole (1.0) | 0.23 ± 0.02 | 0.23 ± 0.02 | 0.29 ± 0.02 | 0.32 ± 0.02 | 0.43 ± 0.04 | 0.49 ± 0.04 | 0.63 ± 0.06 | 0.82 ± 0.03 | 0.19 ± 0.05 |
Norfluoxetine (25) | 0.26 ± 0.03 | 0.18 ± 0.01 | 0.32 ± 0.03 | 0.40 ± 0.04 | 0.47 ± 0.04 | 0.57 ± 0.04 | 0.73 ± 0.01 | 0.83 ± 0.03 | 4.3 ± 1.3 |
Fluvoxamine (50) | 0.49 ± 0.05 | 0.48 ± 0.08 | 0.48 ± 0.06 | 0.50 ± 0.01 | 0.58 ± 0.06 | 0.69 ± 0.05 | 0.75 ± 0.03 | 0.83 ± 0.05 | 37.4 ± 4.7 |
Fluconazole (10) | 0.33 ± 0.02 | 0.36 ± 0.03 | 0.37 ± 0.06 | 0.44 ± 0.07 | 0.51 ± 0.06 | 0.51 ± 0.07 | 0.52 ± 0.04 | 0.54 ± 0.06 |
Table entries (Rv values) are defined from eq. 1 in text.
↵1-150 Parameter estimate ± standard error of estimate from nonlinear regression, based on eq. 5 in text.