TABLE 5

Cytochrome P450 activity (nmol/min) with respect to triazolam 4-hydroxylation and clonazepam 3-hydroxylation in rat microsomes

Values are mean ± S.D. (n = 4).


Time (min)

Triazolam

Clonazepam
0.5 mg/ml
1 mg/ml
2 mg/ml
5 mg/ml
0.5 mg/ml
5 mg/ml
0 0.082 ± 0.027 (100)a 0.13 ± 0.035 (100) 0.16 ± 0.031 (100) 0.18 ± 0.021 (100) 0.041 ± 0.015 (100) 0.10 ± 0.031 (100)
30 0.068 ± 0.021 (83) 0.083 ± 0.018b (66) 0.12 ± 0.029b (74) 0.085 ± 0.024b (47) 0.034 ± 0.013 (83) 0.048 ± 0.0084b (46)
60
0.047 ± 0.014b (58)
0.069 ± 0.016b (55)
0.071 ± 0.013b (44)
0.014 ± 0.0077b (8)
0.027 ± 0.011 (65)

  • a Numbers in parentheses represent a percentage of the time = 0 value.

  • b Significantly different from the corresponding time = 0 value (p < 0.05, Dunnett's test).