TABLE 8

Strong CYP3A inhibitors (oral midazolam used as probe substrate)


Drug

Dose/Regimen

Midazolam Dose

Fold Elevation in Midazolam AUC (GMRa)

Reference
Ketoconazole 400 mg q.d. × 4 days 7.5 mg p.o. 16 Olkkola et al., 1994
Ketoconazole 3 doses of 200 mg 6 mg p.o. 11 Tsunoda et al., 1999
Itraconazole 200 mg q.d. × 4 days 7.5 mg p.o. 11 Olkkola et al., 1994
Mibefradil 100 mg p.o. 2 mg p.o. 8.9 Veronese et al., 1999
Ketoconazole 200 mg q.d. × 11 days Not specified 8.7 Lam et al., 1999
Itraconazole 200 mg q.d. × 4 days 15 or 7.5 mg p.o. 8 Backman et al., 1998
Clarithromycin 500 mg b.i.d. × 7 days 3-4 mg p.o. 7.1 Gorski et al., 1999
Clarithromycin 500 mg b.i.d. × 7 days 4 mg p.o. 7 Gorski et al., 1998
Ketoconazole 200 mg given simultaneously 2 mg p.o. 6.2 Olkkola et al., 1994
Itraconazole 100 mg q.d. × 4 days 7.5 mg p.o. 6 Ahonen et al., 1995
Ketoconazole
200 mg given 2 h before
2 mg p.o.
5
Olkkola et al., 1994
  • a GMR, geometric mean ratio.