Table 4.
In vivo database for the interactions involving CYP2C9
| Substrate | Inhibitor | AUC ratio | Ki(µm) | [I]av/Ki | [I]av,u/Ki | [I]max/Ki | [I]in/Ki | Reference |
|---|---|---|---|---|---|---|---|---|
| S-Warfarin | Amiodarone | 2.11 | 95 | 0.033 | 0.0014 | 0.033 | 0.23 | 4.01 |
| S-Warfarin | Amiodarone | 1.27 | 95 | 0.024 | 0.001 | 0.025 | 0.31 | 4.02 |
| Phenytoin | Amiodarone | 1.40 | 95 | 0.016 | 0.0006 | 0.016 | 0.21 | 4.03 |
| S-Warfarin | Benzbromarone | 2.15 | 0.0085 | 550 | 0.55 | 960 | 1400 | 4.04 |
| S-Warfarin | Bucolome | 3.29 | 20 | 1.9 | 0.19 | 2.4 | 5.3 | 4.05 |
| S-Warfarin | Fluconazole | 2.84 | 7.5 | 6.2 | 5.5 | 8 | 17 | 4.06 |
| Tolbutamide | Fluconazole | 2.09 | 16 | 0.73 | 0.65 | 0.94 | 2 | 4.07 |
| Phenytoin | Fluconazole | 1.75 | 7.5 | 3.2 | 2.8 | 4.1 | 8.6 | 4.08 |
| Phenytoin | Fluconazole | 1.33 | 7.5 | 6.2 | 5.5 | 8 | 17 | 4.09 |
| Losartan | Fluconazole | 1.69 | 13 | 1.8 | 1.6 | 2.4 | 5 | 4.10 |
| Losartan | Fluconazole | 1.27 | 13 | 1.8 | 1.6 | 2.4 | 5 | 4.11 |
| Fluvastatin | Fluconazole | 1.84 | 13 | 1.8 | 1.6 | 2.4 | 5 | 4.12 |
| Glimepiride | Fluconazole | 2.38 | 13 | 1.8 | 1.6 | 2.4 | 5 | 4.13 |
| Diclofenac | Fluvastatin | 1.25 | 0.18 | 0.32 | 0.0032 | 7.1 | 31 | 4.14 |
| Tolbutamide | Fluvastatin | 1.23 | 0.25 | 0.23 | 0.0032 | 5.1 | 22 | 4.15 |
| Tolbutamide | Ketoconazole | 1.77 | 8.1 | 0.65 | 0.0065 | 3.3 | 3.5 | 4.16 |
| Phenprocoumon | Lornoxicam | 1.13 | 12 | 0.1 | 0.001 | 0.24 | 0.22 | 4.17 |
| R-Acenocoumarol | Lornoxicam | 1.06 | 10 | 0.12 | 0.0012 | 0.28 | 0.26 | 4.18 |
| S-Warfarin | Miconazole | 4.72 | 0.5 | 0.54 | 0.054 | 0.75 | 33 | 4.19 |
| Phenytoin | Sertraline | 1.19 | 33 | 0.013 | 0.0001 | 0.018 | 1.1 | 4.20 |
| Tolbutamide | Sertraline | 1.19 | 33 | 0.005 | <0.0001 | 0.0065 | 1.1 | 4.21 |
| Tolbutamide | Sulphamethizole | 1.62 | 75 | 0.0012 | 0.004 | 3.1 | 4.22 | |
| Tolbutamide | Sulphaphenazole | 5.28 | 0.32 | 220 | 70 | 320 | 530 | 4.23 |
| Tolbutamide | Sulphaphenazole | 3.10 | 0.32 | 220 | 70 | 320 | 530 | 4.24 |
| S-Warfarin | Sulphinpyrazone | 1.70 | 230 | 0.018 | 0.0004 | 0.042 | 0.15 | 4.25 |
| S-Warfarin | Sulphinpyrazone | 1.93 | 230 | 0.018 | 0.0004 | 0.042 | 0.15 | 4.26 |
References for Table 4
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