Effects of cimetidine and probenecid treatments on pharmacokinetic parameters of fexofenadine
Parameter | Control | Cimetidine | Probenecid |
|---|---|---|---|
| AUC(0-∞) (ng · h/ml) | 3637 ± 1199 | 4124 ± 2019 | 6150 ± 3972 |
| Ratio to control | 1 | 1.08 | 1.53 |
| CLrenal, u (ml/min)a | 230 ± 78 | 152 ± 70 | 74 ± 52 |
| Ratio to control | 1 | 0.610 | 0.270 |
| CLsc (ml/min)b | 133 | 55.0 | 0 (almost) |
| Ratio to control | 1 | 0.414 | 0 (almost) |
| I u, max c | 5.20 | 24.0 | |
| Ki (Km) for hOAT3 | (113) | 1.30 | |
|
R
d
|
| 0.956 | 0.0514 |
↵ a CLrenal, u, unbound renal clearance (Yasui-Furukori et al., 2005).
↵ b CLsc, tubular secretion clearance (CLrenal, u - CLcreatinine). Creatinine clearance value was used for the value of glomerular filtration rate (97 ml/min; van Crugten et al., 1985).
↵ c Iu, max, maximum unbound plasma concentration of inhibitor (Selen et al., 1982; van Crugten et al., 1985).
↵ d R value was calculated according to the following equation: R = 1/(1 + Iu, max/Ki).