Microsomal and hepatocyte in vitro intrinsic clearance values for the 29 drugs examined (Obach, 1999)
| Drug | CLint1-a | |
|---|---|---|
| Microsomal | Hepatocyte | |
| ml/min/kg | μl/min/million cells | |
| Basic compounds | ||
| Chlorpromazine | 25 ± 61-b | 10.41-c |
| Propafenone | 166 ± 8 | 69.2 |
| Verapamil | 122 ± 2 | 50.8 |
| Diphenhydramine | 2.1 ± 0.9 | 0.9 |
| Lorcainide | 50 ± 6 | 20.8 |
| Diltiazem | 15 ± 2 | 6.2 |
| Amitriptyline | 14 ± 2 | 5.8 |
| Desipramine | 17 ± 7 | 7.1 |
| Imipramine | 19 ± 2 | 7.9 |
| Ketamine | 27 ± 4 | 11.2 |
| Quinidine | 3.4 ± 0.5 | 1.4 |
| Clozapine | 4.6 ± 0.9 | 1.9 |
| Neutral compounds | ||
| Dexamethasone | 3.0 ± 0.2 | 1.2 |
| Prednisone1-d | 2.7 ± 0.0 | 1.1 |
| Diazepam | 2.3 ± 0.7 | 0.9 |
| Midazolam | 160 ± 3 | 66.7 |
| Methoxsalen | 40 ± 3 | 16.7 |
| Alprazolam1-d | 1.6 ± 1.0 | 0.7 |
| Triazolam | 19 ± 1 | 7.9 |
| Zolpidem | 2.8 ± 0.3 | 1.2 |
| Diclofenac | 189 ± 39 | 78.7 |
| Acidic compounds | ||
| Ibuprofen1-d | 8.8 ± 0.9 | 3.7 |
| Tolbutamide | 0.90 ± 0.15 | 0.4 |
| Warfarin | <0.52 | 0.2 |
| Tenidap | 8.3 ± 0.7 | 3.4 |
| Tenoxicam | 1.7 ± 0.4 | 0.7 |
| Amobarbital | 0.94 ± 0.07 | 0.4 |
| Hexobarbital | 2.3 ± 0.3 | 0.9 |
| Methohexital | 49 ± 8 | 20.4 |
↵1-a CLint, intrinsic clearance.
↵1-b Each value represents the mean ± S.D. for triplicate determinations. Intrinsic clearance values were calculated from in vitro t1/2 data as described previously (Obach, 1999).
↵1-c Calculated using 20 g of liver/kg and 120 million hepatocytes/g of liver as described underMaterials and Methods.
↵1-d Molecules used as an external test set.