Victim Drug | EH | fm, CYPi | fhep | FG | AUC′IV/AUCIV Error ≥±30% | Clint, GI′/Clint, GI Error ≥±30% | Ignoring EH for Determination of fm, CYPi | |||
---|---|---|---|---|---|---|---|---|---|---|
Inhibition I/Ki or λ/kdeg ≥ | Fold Induction ≥ | Inhibition I/Ki or λ/kdeg ≥ | Fold Induction ≥ | fm, CYPi Ignoring EH | %Error in Maximum Oral AUC Ratio (−fm, CYPi · EH · 100) | |||||
CYP3A | ||||||||||
Midazolam | 0.44a | 0.93b | 0.995c | 0.54a | 1.3 | 2.1 | 0.37 | 1.5 | 0.90 | −41 |
Alfentanil | 0.28d | 0.98d | 0.99 | 0.59d | 9.0 | 2.6 | 0.54 | 1.6 | 0.96 | −27 |
Nifedipine | 0.45b | 0.78e | 0.99 | 0.74b | 2.0 | 2.3 | 0.25 | 1.3 | 0.65 | −35 |
CYP2C9 | ||||||||||
Tolbutamide | 0.01f | 0.78b | 1 | N.A. | Not possible | 56 | N.A. | 0.78 | −0.8 | |
S-Warfarin | 0.003g | 0.91b | 1 | N.A. | Not possible | 160 | N.A. | 0.91 | −0.3 | |
CYP2D6 | ||||||||||
Desipramine | 0.48h | 0.88i | 1 | N.A. | 0.9 | 2.0 | N.A. | 0.79 | −42 | |
Imipramine | 0.70j | 0.46i | 1 | N.A. | 2.6 | 2.3 | N.A. | 0.20 | −32 | |
Metoprolol | 0.84k | 0.83i | 1 | N.A. | 0.5 | 1.6 | N.A. | 0.44 | −70 | |
Propranolol | 0.62l | 0.37i | 1 | N.A. | Not Possible | 2.9 | N.A. | 0.18 | −23 |
N.A., not applicable.
↵a Data from Thummel et al. (1996).
↵b Data from Obach et al. (2006).
↵c Data from Midazolam HCL Injection package insert (Baxter Healthcare, Deerfield, IL).
↵d Data from Kharasch et al. (2004).
↵e Data from Ohno et al. (2007).
↵f Data from Miners et al. (1982).
↵g Data from Abernethy et al. (1991).
↵h Data from Ciraulo et al. (1988).
↵i Data from Ito et al. (2005).
↵j Data from Abernethy et al. (1984).
↵k Data from Leemann et al. (1993).
↵l Data from Feely et al. (1981).