Table 3.
Substrate | Inhibitor | AUC ratio | Ki* (µm) | [I]av/Ki | [I]av,u/Ki | [I]max/Ki | [I]in/Ki | Reference |
---|---|---|---|---|---|---|---|---|
Midazolam | Azithromycin | 0.87 | 30 | 0.0046 | 0.0033 | 0.0056 | 0.71 | 3.01 |
Midazolam | Azithromycin | 1.19 | 30 | 0.0092 | 0.0066 | 0.011 | 1.4 | 3.02 |
Midazolam | Clarithromycin | 3.57 | 57 | 0.0087 | 0.0047 | 0.024 | 0.37 | 3.02 |
Triazolam | Azithromycin | 1.03 | 30 | 0.0092 | 0.0066 | 0.01 | 0.71 | 3.03 |
Triazolam | Clarithromycin | 5.06 | 57 | 0.017 | 0.0094 | 0.048 | 0.74 | 3.03 |
Triazolam | Erythromycin | 3.65 | 77 | 0.0068 | 0.0011 | 0.035 | 0.56 | 3.03 |
Midazolam | Azithromycin | 1.27 | 30 | 0.0092 | 0.0066 | 0.011 | 1.4 | 3.04 |
Midazolam | Erythromycin | 3.81 | 170 | 0.0046 | 0.0004 | 0.016 | 0.25 | 3.04 |
Alprazolam | Cimetidine | 1.58 | 140 | 0.034 | 0.028 | 0.081 | 0.56 | 3.05 |
Triazolam | Cimetidine | 1.54 | 99 | 0.048 | 0.039 | 0.11 | 0.8 | 3.05 |
Alprazolam | Cimetidine | 1.73 | 140 | 0.028 | 0.023 | 0.067 | 0.38 | 3.06 |
Triazolam | Cimetidine | 2.20 | 99 | 0.04 | 0.033 | 0.096 | 0.54 | 3.06 |
Midazolam | Cimetidine | 2.02 | 180 | 0.022 | 0.0089 | 0.052 | 0.29 | 3.07 |
Midazolam | Ranitidine | 1.66 | 170 | 0.0027 | 0.0012 | 0.011 | 0.17 | 3.07 |
Midazolam | Cimetidine | 1.35 | 180 | 0.018 | 0.0071 | 0.074 | 0.56 | 3.08 |
Midazolam | Ranitidine | 1.23 | 170 | 0.0027 | 0.0012 | 0.011 | 0.17 | 3.08 |
Nifedipine | Cimetidine | 1.60 | 140 | 0.028 | 0.023 | 0.24 | 1.8 | 3.09 |
Nifedipine | Ranitidine | 1.22 | 170 | 0.0027 | 0.0023 | 0.011 | 0.17 | 3.09 |
Nifedipine | Cimetidine | 2.01 | 140 | 0.023 | 0.018 | 0.19 | 1.4 | 3.10 |
Nifedipine | Ranitidine | 1.06 | 170 | 0.0055 | 0.0047 | 0.022 | 0.35 | 3.10 |
Nimodipine | Cimetidine | 1.74 | 140 | 0.028 | 0.023 | 0.067 | 0.38 | 3.11 |
Nimodipine | Ranitidine | 0.99 | 170 | 0.0027 | 0.0023 | 0.022 | 0.35 | 3.11 |
Nisoldipine | Cimetidine | 1.49 | 140 | 0.028 | 0.023 | 0.067 | 0.38 | 3.12 |
Nitrendipine | Cimetidine | 2.41 | 140 | 0.027 | 0.022 | 0.057 | 0.38 | 3.13 |
Triazolam | Cimetidine | 1.55 | 99 | 0.048 | 0.039 | 0.11 | 0.8 | 3.14 |
Triazolam | Cimetidine | 1.32 | 99 | 0.048 | 0.039 | 0.11 | 0.8 | 3.15 |
Midazolam | Clarithromycin | 7.00 | 57 | 0.017 | 0.0094 | 0.048 | 0.74 | 3.16 |
Lovastatin | Cyclosporin | 1.89 | 2 | 0.059 | 0.0041 | 0.11 | 3.7 | 3.17 |
Buspirone | Diltiazem | 5.50 | 65 | 0.0024 | 0.0005 | 0.0047 | 0.14 | 3.18 |
Buspirone | Verapamil | 3.40 | 16 | 0.0047 | 0.0005 | 0.0087 | 0.68 | 3.18 |
Cyclosporin | Diltiazem | 1.49 | 63.0 | 0.0033 | 0.0007 | 0.0084 | 0.29 | 3.19 |
Cyclosporin | Diltiazem | 1.57 | 63.0 | 0.0025 | 0.0006 | 0.0063 | 0.22 | 3.20 |
Cyclosporin | Ketoconazole | 4.39 | 0.37 | 1.2 | 0.012 | 6.2 | 66 | 3.20 |
Lovastatin | Diltiazem | 3.57 | 65 | 0.0032 | 0.0007 | 0.0081 | 0.28 | 3.21 |
Midazolam | Diltiazem | 3.75 | 54 | 0.0029 | 0.0003 | 0.0056 | 0.17 | 3.22 |
Midazolam | Verapamil | 2.92 | 13 | 0.0061 | 0.0003 | 0.011 | 0.87 | 3.22 |
Nifedipine | Diltiazem | 2.22 | 65 | 0.0012 | 0.0003 | 0.0023 | 0.07 | 3.23 |
Nifedipine | Diltiazem | 3.11 | 65 | 0.0036 | 0.0008 | 0.007 | 0.21 | 3.23 |
Simvastatin | Diltiazem | 4.82 | 65 | 0.0032 | 0.0007 | 0.0081 | 0.28 | 3.24 |
Triazolam | Diltiazem | 3.38 | 54 | 0.0029 | 0.0006 | 0.0056 | 0.17 | 3.25 |
Triazolam | Diltiazem | 2.30 | 54 | 0.0029 | 0.0006 | 0.0056 | 0.17 | 3.26 |
Alprazolam | Erythromycin | 2.47 | 120 | 0.005 | 0.0008 | 0.018 | 0.28 | 3.27 |
Buspirone | Erythromycin | 5.90 | 110 | 0.0075 | 0.0012 | 0.027 | 0.41 | 3.28 |
Buspirone | Itraconazole | 19.20 | 0.91 (2.2) | 0.26 | 0.0005 | 0.32 | 9.9 | 3.28 |
Cerivastatin | Erythromycin | 1.21 | 110 | 0.0075 | 0.0012 | 0.027 | 0.41 | 3.29 |
Cyclosporin | Erythromycin | 2.22 | 66 | 0.0079 | 0.0013 | 0.022 | 0.33 | 3.30 |
Cyclosporin | Erythromycin | 2.15 | 66 | 0.016 | 0.0025 | 0.044 | 0.66 | 3.31 |
Felodipine | Erythromycin | 2.49 | 110 | 0.005 | 0.0008 | 0.014 | 0.21 | 3.32 |
Midazolam | Erythromycin | 4.42 | 170 | 0.0046 | 0.0004 | 0.016 | 0.25 | 3.33 |
Quinidine | Erythromycin | 1.19 | 110 | 0.005 | 0.0008 | 0.014 | 0.21 | 3.34 |
Quinidine | Itraconazole | 2.58 | 0.91 (2.2) | 0.13 | 0.0003 | 0.19 | 9.8 | 3.34 |
Simvastatin | Erythromycin | 6.20 | 110 | 0.0075 | 0.0012 | 0.023 | 0.41 | 3.35 |
Simvastatin | Verapamil | 4.60 | 16 | 0.0047 | 0.0005 | 0.0087 | 0.68 | 3.35 |
Triazolam | Erythromycin | 2.06 | 120 | 0.0042 | 0.0007 | 0.015 | 0.23 | 3.36 |
Quinidine | Felodipine | 1.07 | 11 | 0.0003 | <0.0001 | 0.0005 | 0.15 | 3.37 |
Quinidine | Nifedipine | 1.15 | 17 | 0.0047 | 0.0002 | 0.022 | 0.21 | 3.37 |
Cyclosporin | Fluconazole | 1.84 | 40 | 0.54 | 0.48 | 0.69 | 1.55 | 3.38 |
Midazolam | Fluconazole | 3.60 | 6 | 3.6 | 1.6 | 4.6 | 10 | 3.39 |
Midazolam | Itraconazole | 6.64 | 0.92 (6.3) | 0.18 | 0.0004 | 0.26 | 19 | 3.39 |
Rifabutin | Fluconazole | 1.82 | 12 | 1.8 | 1.6 | 2.3 | 5.2 | 3.40 |
Triazolam | Fluconazole | 1.63 | 1.8 | 2.9 | 2.6 | 3.8 | 8.5 | 3.41 |
Triazolam | Fluconazole | 2.05 | 1.8 | 5.9 | 5.2 | 7.6 | 17 | 3.41 |
Triazolam | Fluconazole | 4.42 | 1.8 | 12 | 10 | 15 | 34 | 3.41 |
Triazolam | Fluconazole | 2.46 | 1.8 | 5.9 | 5.2 | 7.6 | 17 | 3.42 |
Triazolam | Terbinafine | 0.81 | 100 | 0.012 | <0.0001 | 0.02 | 0.55 | 3.42 |
Alprazolam | Fluoxetine | 1.34 | 65 (10) | 0.088 | 0.0053 | 0.1 | 0.27 | 3.43 |
Alprazolam | Fluoxetine | 1.26 | 65 (10) | 0.059 | 0.0035 | 0.063 | 0.12 | 3.44 |
Triazolam | Fluoxetine | 1.02 | 26 (5.4) | 0.14 | 0.0085 | 0.16 | 0.61 | 3.45 |
Alprazolam | Fluvoxamine | 1.96 | 9.2 | 0.035 | 0.0080 | 0.057 | 2.2 | 3.46 |
Buspirone | Fluvoxamine | 2.35 | 11 | 0.029 | 0.0066 | 0.048 | 1.8 | 3.47 |
Quinidine | Fluvoxamine | 1.41 | 11 | 0.029 | 0.0066 | 0.048 | 1.8 | 3.48 |
Triazolam | Isradipine | 0.80 | 17 | 0.0001 | <0.0001 | 0.0003 | 0.043 | 3.49 |
Triazolam | Mibefradil | 8.97 | 2.5 | 0.25 | 0.001 | 0.39 | 2.8 | 3.49 |
Alprazolam | Itraconazole | 2.66 | 0.95 (2.2) | 0.26 | 0.0005 | 0.37 | 19 | 3.50 |
Astemizole | Itraconazole | 2.77 | 0.91 (2.2) | 0.52 | 0.001 | 0.63 | 20 | 3.51 |
Atorvastatin | Itraconazole | 3.64 | 0.91 (2.2) | 0.26 | 0.0005 | 0.38 | 20 | 3.52 |
Buspirone | Itraconazole | 14.50 | 0.91 (2.2) | 0.26 | 0.0005 | 0.38 | 20 | 3.53 |
Cerivastatin | Itraconazole | 1.15 | 0.91 (2.2) | 0.26 | 0.0005 | 0.38 | 20 | 3.54 |
Felodipine | Itraconazole | 6.34 | 0.91 (2.2) | 0.26 | 0.0005 | 0.38 | 20 | 3.55 |
Lovastatin | Itraconazole | 22.10 | 0.91 (2.2) | 0.26 | 0.0005 | 0.38 | 20 | 3.56 |
Lovastatin | Itraconazole | 15.40 | 0.91 (2.2) | 0.13 | 0.0003 | 0.19 | 9.8 | 3.57 |
Midazolam | Itraconazole | 7.97 | 0.92 (6.3) | 0.18 | 0.0004 | 0.26 | 19 | 3.58 |
Midazolam | Itraconazole | 5.75 | 0.92 (6.3) | 0.089 | 0.0002 | 0.13 | 9.7 | 3.59 |
Midazolarn | Itraconazole | 10.80 | 0.92 (6.3) | 0.36 | 0.0007 | 0.52 | 39 | 3.60 |
Midazolam | Ketoconazole | 15.90 | 0.088 | 5 | 0.025 | 26 | 270 | 3.60 |
Quinidine | Itraconazole | 2.42 | 0.91 (2.2) | 0.26 | 0.0005 | 0.38 | 20 | 3.61 |
Simvastatin | Itraconazole | 18.60 | 0.91 (2.2) | 0.26 | 0.0005 | 0.38 | 20 | 3.62 |
Triazolam | Itraconazole | 27.10 | 0.16 (0.2) | 2.2 | 0.0044 | 3.2 | 110 | 3.63 |
Triazolam | Ketoconazole | 22.40 | 0.022 | 41 | 0.41 | 210 | 2200 | 3.63 |
Alprazolam | Ketoconazole | 3.98 | 0.061 | 15 | 0.15 | 40 | 400 | 3.64 |
Triazolam | Ketoconazole | 13.70 | 0.022 | 41 | 0.41 | 110 | 1100 | 3.64 |
Cyclosporin | Ketoconazole | 5.15 | 0.36 | 2.5 | 0.025 | 6.7 | 67 | 3.65 |
Cyclosporin | Ketoconazole | 5.31 | 0.36 | 1.2 | 0.012 | 6.2 | 66 | 3.66 |
Midazolam | Ketoconazole | 16.00 | 0.088 | 10 | 0.051 | 28 | 280 | 3.67 |
Nisoldipine | Ketoconazole | 24.40 | 0.099 | 4.5 | 0.045 | 23 | 240 | 3.68 |
Tacrolimus | Ketoconazole | 2.88 | 8 | 0.056 | 0.0006 | 0.28 | 3 | 3.69 |
Triazolam | Ketoconazole | 9.16 | 0.022 | 31 | 0.31 | 110 | 1100 | 3.70 |
Alprazolam | Nefazodone | 1.41 | 1.2 | 0.98 | 0.0089 | 2 | 24 | 3.71 |
Triazolam | Nefazodone | 3.90 | 1.2 | 0.98 | 0.0089 | 2 | 24 | 3.72 |
Cyclosporin | Nifedipine | 0.88 | 10 | 0.008 | 0.0003 | 0.037 | 0.36 | 3.73 |
Cyclosporin | Verapamil | 1.45 | 24 | 0.0036 | 0.0004 | 0.0066 | 0.51 | 3.73 |
Quinidine | Nifedipine | 0.98 | 17 | 0.0071 | 0.0003 | 0.023 | 0.21 | 3.74 |
Nifedipine | Quinidine sulphate | 1.37 | 160 | 0.019 | 0.0025 | 0.029 | 0.26 | 3.74 |
Midazolam | Ranitidine | 1.66 | 170 | 0.0027 | 0.0012 | 0.011 | 0.17 | 3.75 |
Alprazolam | Ritonavir | 2.48 | 0.065 | 71 | 1.4 | 120 | 340 | 3.76 |
Midazolam | Roxithromycin | 1.47 | 110 | 0.061 | 0.0012 | 0.19 | 0.26 | 3.77 |
Midazolam | Saquinavir | 5.14 | 3.5 | 0.12 | 0.0012 | 0.15 | 32 | 3.78 |
Quinidine | Verapamil | 1.47 | 16 | 0.0047 | 0.0005 | 0.0087 | 0.68 | 3.79 |
Quinidine | Verapamil | 1.50 | 16 | 0.0071 | 0.0007 | 0.013 | 1 | 3.79 |
*Numbers in parentheses represent the values for metabolites.
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