TABLE 9

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