TABLE 11

Drugs without CYP3A inhibitory activity (oral midazolam used as probe substrate)


Drug

Dose/Regimen

Midazolam Dose

Fold Elevation in Midazolam AUC (GMR)

Reference
Azithromycin 400 mg q.d. × 3 days 15 mg p.o. 1.3 Zimmermann et al., 1996
Cimetidine 800 mg p.o. × 1 day Not noted 1.3 Fee et al., 1987
Simvastatin 80 mg q.d. × 7 days 2 mg p.o. 1.1 Prueksaritanont et al., 2000
Fluoxetine 60 mg q.d. × 5 days, then 20 mg/day Not specified 0.8 Lam et al., 1999
Rifampicin 600 mg q.d. × 5 days 15 mg p.o. 0.023 Backman et al., 1998
Azithromycin 500 mg q.d. × 3 days 15 mg p.o. NSDa Yeates et al., 1996
Terbinafine 250 mg q.d. × 4 days 7.5 mg p.o. NSD Olkkola et al., 1994
Azithromycin
500 mg day 1250 mg days 2-5
15 mg p.o. days
NSD
Backman et al., 1995
  • a NSD, no significant difference in midazolam plasma AUC, with vs. without the interacting drug (GMR ≅ 1.0).