TABLE 1.
Victim Drug | EH | f m, CYPi | f hep | F G | 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 | 0.44 a | 0.93 b | 0.995 c | 0.54 a | 1.3 | 2.1 | 0.37 | 1.5 | 0.90 | −41 |
Alfentanil | 0.28 d | 0.98 d | 0.99 | 0.59 d | 9.0 | 2.6 | 0.54 | 1.6 | 0.96 | −27 |
Nifedipine | 0.45 b | 0.78 e | 0.99 | 0.74 b | 2.0 | 2.3 | 0.25 | 1.3 | 0.65 | −35 |
CYP2C9 | ||||||||||
Tolbutamide | 0.01 f | 0.78 b | 1 | N.A. | Not possible | 56 | N.A. | 0.78 | −0.8 | |
S-Warfarin | 0.003 g | 0.91 b | 1 | N.A. | Not possible | 160 | N.A. | 0.91 | −0.3 | |
CYP2D6 | ||||||||||
Desipramine | 0.48 h | 0.88 i | 1 | N.A. | 0.9 | 2.0 | N.A. | 0.79 | −42 | |
Imipramine | 0.70 j | 0.46 i | 1 | N.A. | 2.6 | 2.3 | N.A. | 0.20 | −32 | |
Metoprolol | 0.84 k | 0.83 i | 1 | N.A. | 0.5 | 1.6 | N.A. | 0.44 | −70 | |
Propranolol | 0.62 l | 0.37 i | 1 | N.A. | Not Possible | 2.9 | N.A. | 0.18 | −23 |
N.A., not applicable.
Data from Thummel et al. (1996).
Data from Obach et al. (2006).
Data from Midazolam HCL Injection package insert (Baxter Healthcare, Deerfield, IL).
Data from Kharasch et al. (2004).
Data from Ohno et al. (2007).
Data from Miners et al. (1982).
Data from Abernethy et al. (1991).
Data from Ciraulo et al. (1988).
Data from Ito et al. (2005).
Data from Abernethy et al. (1984).
Data from Leemann et al. (1993).
Data from Feely et al. (1981).