Relative P450 contribution (fm) to the hepatic metabolism, ketoconazole dose, and estimated Cmax
Compound | fm | Ketoconazole Dosea | Cmax b | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| CYP1A2 | CYP2C9 | CYP2C19 | CYP2D6 | CYP3A4/5 | |||||||
| mg | μM | ||||||||||
| Theophylline | 1 | NA | NA | NA | NA | 200 b.i.d. | 10 | ||||
| Desipramine | NA | NA | NA | 1 | NA | 200 q.d. | 10 | ||||
| Midazolam | NA | NA | NA | NA | 0.94 | 400 q.d. | 20 | ||||
| Tolbutamide | NA | 0.72 | 0.28 | NA | NA | 200 q.d. | 10 | ||||
| Omeprazole | NA | NA | 0.60 | NA | 0.40 | 50–200 q.d. | 2.5–10 | ||||
| Loratadine | NA | NA | NA | NA | 0.60 | 200 b.i.d. | 10 | ||||
| Cyclosporine | NA | NA | NA | NA | 0.71 | 200 q.d. | 10 | ||||
| Alprazolam | NA | NA | NA | NA | 0.80 | 200 b.i.d. | 10 | ||||
| Budesonide | 0.08 | 0.02 | 0 | 0 | 0.79 | 200 q.d. | 10 | ||||
| Buprenorphine | 0.07 | 0.10 | 0 | 0.01 | 0.77 | 200 b.i.d. | 10 | ||||
| Docetaxel | 0.12 | 0 | 0 | 0.18 | 0.70 | 200 q.d. | 10 | ||||
| Loratadine | 0.16 | 0.18 | 0 | 0.24 | 0.41 | 200 b.i.d. | 10 | ||||
| Methylprednisolone | 0 | 0 | 0.10 | 0.31 | 0.59 | 200 q.d. | 10 | ||||
| Sirolimus | 0 | 0.15 | 0 | 0 | 0.85 | NA | 10 | ||||
| Tacrolimus | 0 | 0.08 | 0 | 0.01 | 0.47 | 400 q.d. | 20 | ||||