Compound | Humans | Rats | Urinary Excretion in Humans | Blood/Plasma Ratio | ||
---|---|---|---|---|---|---|
Dose (i.v./oral) | fup | Dose (i.v./oral) | fupa | |||
mg | mg | % of dose | ||||
Alprazolam | 1/1 | 0.29b | 0.467/2.67 | NA | 20c | 0.85d |
Atorvastatin | NA | NA | 0.55/2.75 | 0.045 | NA | 0.61e |
Buspirone | 1/20 | 0.050f | 0.289/0.964 | 0.208 | <0.1c | 0.81e |
Cyclosporine A | 111/372 | 0.068b | 1.13/1.13 | NA | <1c | 1.36e |
Erythromycin | 500/500 | 0.1b | NA | NA | NA | NA |
Felodipine | 3/15 | 0.004c | NA | NA | <1c | 0.70e |
Indinavir | NA | NA | 1.75/7 | 0.360b | NA | 0.84e |
Midazolam | 5/10 | 0.020c | 2.25/3.38 | 0.046 | <1 | 0.75e |
Nifedipine | 1.46/20 | 0.058 | 1.65/1.68 | 0.033 | 0c | 0.67d |
Paracetamol | 1000/500 | 0.75b | 33.3/33.3 | 0.492 | NA | NA |
Saquinavir | 12/600 | 0.020g | NA | NA | NA | 0.74e |
Sildenafil | 50/50 | 0.065 | 2.82/8.97 | 0.103 | NA | 0.64d |
Tacrolimus | 1.55/3.88 | 0.012h | 0.425/2.13 | NA | NA | 35e |
Terfenadine | NA/60 | 0.01 | NA | <0.05 | NA | 1e |
Triazolam | 0.25/0.25 | 0.145 | NA | NA | NA | 0.62d |
Verapamil | 10/120 | 0.105 | 1.18/1.18 | 0.153 | NA | 0.89d |
NA, not applicable.
↵a When no data were available for fup in rat plasma, the corresponding value in humans was used.
↵b Data are from Obach et al., 2008.
↵c Data are from Goodman et al., 2006.
↵d Data are from Gertz et al., 2010.
↵e Data are from Gertz et al., 2011.
↵f Data are from Gammans et al., 1986.
↵g Data are from Wishart et al., 2008.
↵h Data are from Zahir et al., 2001.