TABLE 3

Data for human microsome incubations corrected for both fub and fuinc


Compound

Chemical Class

Human Liver Microsomal CLint, in vitro

CLint, ub, in vivo
Predicted
Observed
μl/min/mg ml/min/kg
Alprazolama N 1.6 2.4 1.9
Amitryptylinea B 14 94.3 516.0
Amobarbitala A 0.94 1.2 1.4
Chlorpromazinea B 25 229.6 381.3
Clozapinea B 4.6 35.7 59.0
Desipraminea B 17 81.8 160.0
Dexamethasonea N 3 3.0 13.6
Diazepamb N 3 11.8 28.0
Diclofenacb A 378.02 183.8 1667.3
Diltiazemc B 33.5 77.7 232.6
Diphenhydraminea B 2.10 7.3 53.5
FK1052d N 58.3 182.0 1525.0
FK480d N 73.5 662.0 327.3
Fluvastatine A 47.06 75.4 1052.0
Hexobarbitala A 2.3 2.9 8.3
Ibuprofenb A 21.79 12.3 102.4
Imipraminea B 19 106.6 330.0
Lorcainidea B 50 97.1 924.0
Methohexitala A 49 57.6 207.4
Methoxsalena N 40 43.0 1340.0
Metoprololc B 5 6.8 20.2
Midazolama N 160 183.7 163.2
Nicardipined N 1719 13460.0 1806.7
Nilvadipined N 1695 3867.0 8123.4
Omeprazoled N 97.1 101.0 502.7
Phenacetinc N 9 9.9 212.5
Phenytoinf A 0.18 0.5 4.0
Prednisonea N 2.7 13.6 21.5
Propafenonea B 166 644.9 6650.0
Propranololc B 13 16.3 284.5
Quinidinea B 3.4 10.7 22.1
Tenidapa A 8.3 26.2 80.4
Tenoxicama A 1.7 2.2 2.2
Tolbutamideb A 1.94 1.3 6.4
Triazolama N 19 24.6 38.1
Verapamilb B 122 553.6 935.3
Zolpidemd
N
28.7
17.9
115.5
  • A, acid; B, base; N, neutral.

    Data were obtained from a Obach (1999); b mean data (see Table 5); c this laboratory; d Naritomi et al. (2001); e Andersson et al. (2004); f Carlile et al. (1999).