Moderate CYP3A inhibitors (oral midazolam used as probe substrate)
Drug | Dose/Regimen | Midazolam Dose | Fold Elevation in Midazolam AUC (GMR) | Reference |
|---|---|---|---|---|
| Erythromycin | 500 mg t.i.d. × 7 days | 15 mg p.o. | 4.4 | Olkkola et al., 1993 |
| Erythromycin | 500 mg t.i.d. × 5 days | 15 mg p.o. | 3.8 | Zimmermann et al., 1996 |
| Diltiazem | 60 mg t.i.d. × 2 days | 15 mg p.o. | 3.7 | Backman et al., 1994b (Versed package circular, 2001) |
| Clarithromycin | 250 mg b.i.d. × 5 days | 15 mg p.o. | 3.6 | Yeates et al., 1996 |
| Fluconazole | 400 mg p.o. | 7.5 mg p.o. | 3 | Ahonen et al., 1997 |
| Fluconazole | 400 mg i.v. | 7.5 mg p.o. | 3 | Ahonen et al., 1997 |
| Verapamil | 80 mg t.i.d. × 2 days | 15 mg p.o. | 2.9 | Backman, et al., 1994b (Versed package circular, 2001) |
| Grapefruit Juice | 8 oz with breakfast × 4 days | 2 mg p.o. | 2.4 | Rogers et al., 1999 |
|
Grapefruit Juice
|
8 oz with breakfast × 4 days
|
2 mg p.o.
|
2.4
|
Blum et al., 1999
|