TABLE 1

CYP3A4 inhibitor ketoconazole with midazolam used as probe substrate in healthy volunteers


Ketoconazole Dosage Regimen

Midazolam Dosage Regimen

-Fold Elevation in Midazolam Exposure

Reference
400 mg q.d. × 4 days 7.5 mg p.o. 16 Olkkola et al., 1994
3 doses of 200 mg 6 mg p.o. 16 Tsunoda et al., 1999
3 doses of 200 mg 2 mg i.v. 5 Tsunoda et al., 1999
200 mg q.d. × 11 days Not specified 8.7 Lam et al., 1999
200 mg given simultaneously 2 mg p.o. 6.2 Olkkola et al., 1994
200 mg given before 2 mg p.o. 5 Olkkola et al., 1994
3 doses of 200 mg 5 mg p.o. 5 Lee et al., 2002
200 mg q.d. × 12 days 10 mg p.o. 7 Lam et al., 2003
400 mg q.d. × 10 days
5.5 mg p.o.
10
Chung et al., 2006