Table 2

Correlation of the metabolism of carvedilol with other P450 related activities in human liver microsomes from 26 human livers

CYPEnzyme Activityt2-a
4OHC5OHC8OHCODMC
R(+)-carvedilol
1A2Caffeine N3-demethylaseNRNRNRNR
2A6Coumarin 7-hydroxylaseNRNRNRNR
2C9Tolbutamide hydroxylaseNRNRNR2.32*
2C19S-mephenytoin 4-hydroxylaseNRNRNRNR
2D6Bufurolol 1′-hydroxylase 4.56***  9.24*** NR4.24**
2E1Lauric acid ω-1 hydroxylaseNR 3.97** NR2.31*
3ACyclosporine oxidaseNRNR4.56*** NR
4ALauric acid ω-hydroxylaseNRNRNRNR
S(−)-carvedilol
1A2Caffeine N3-demethylaseNRNR3.38* NR
2A6Coumarin 7-hydroxylaseNRNRNRNR
2C9Tolbutamide hydroxylase 3.62** NRNR5.29***
2C19S-mephenytoin 4-hydroxylaseNRNRNRNR
2D6Bufurolol 1′-hydroxylase15.44*** 12.23*** NR2.77*
2E1Lauric acid ω-1 hydroxylaseNR 3.14* NRNR
3ACyclosporine oxidaseNRNR3.83** NR
4ALauric acid ω-hydroxylaseNR 2.09* NRNR
  • 2-a t-statistic for the null hypothesis that the coefficient of the model is zero.

  • * p < 0.05; ** p < 0.001; *** p < 0.0001.

  • NR, No or negative relationship in the model.