Disposition of terfenadine in control and DEX-treated (100 μM; 48 h) day 4 SC rat hepatocytes The amount (nanomoles) of terfenadine and the metabolites fexofenadine and azacyclonol in medium and hepatocytes (cells + BC) after incubation of terfenadine (5 μM) is shown. Data represent mean \m=+-\ S.D. of three individual experiments.
Time | TER | FEX | AZA | Total | Recovery | |||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Medium | Cells + BC | Medium | Cells + BC | Medium | Cells + BC | |||||||||
h | nmol | nmol | % | |||||||||||
Control | 1 | 5.6 ± 1.6 | 3.7 ± 0.3 | 1.0 ± 0.4 | 1.5 ± 0.5 | 0.16 ± 0.08 | 0.15 ± 0.05 | 12 ± 3 | 81 ± 18 | |||||
2 | 3.6 ± 0.7* | 2.1 ± 0.9 | 2.8 ± 0.7* | 1.6 ± 0.2 | 0.21 ± 0.09 | 0.15 ± 0.02 | 10 ± 0.9 | 64 ± 6 | ||||||
4 | 0.5 ± 0.1* | 1.6 ± 0.6 | 5.6 ± 0.8* | 1.3 ± 0.2 | 0.22 ± 0.07 | 0.11 ± 0.03 | 10 ± 0.1 | 67 ± 7 | ||||||
DEX-treated | 1 | 3.1 ± 0.4† | 2.1 ± 0.3† | 1.8 ± 0.4 | 1.3 ± 0.3 | 1.1 ± 0.04† | 1.3 ± 0.3† | 10 ± 2 | 73 ± 15 | |||||
2 | 1.1 ± 0.0*† | 1.1 ± 0.2 | 4.5 ± 0.7† | 0.8 ± 0.1† | 1.6 ± 0.2† | 2.2 ± 0.7† | 11 ± 2 | 74 ± 13 | ||||||
| 4 | <LLOQ | 0.3 ± 0.1 | 6.5 ± 0.7† | 0.6 ± 0.1*† | 2.3 ± 0.3*† | 1.3 ± 0.0† | 11 ± 2 | 74 ± 12 |