TABLE 2

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
  • <LLOQ, below the lower limit of quantitation

  • * P < 0.05 vs. 1 h (same treatment)

  • P < 0.05 vs. control (same time point)