IC50 values for inhibition of human liver microsomal R- and S-lorazepam glucuronidation
Data are given as IC50 ± standard error of parameter fit. The unbound concentration range of each inhibitor (i.e., corrected for nonspecific binding to HLM) is shown in parentheses.
| Inhibitor | IC50 | |
|---|---|---|
| R-Lorazepam | S-Lorazepam | |
| µM | µM | |
| Codeine (10–1000 µM) | 809 ± 0.4 | 2562 ± 277 |
| Fluconazole (10–1000 µM) | 4599 ± 315 | 4245 ± 19 |
| Ketamine (10–1000 µM) | 205 ± 2 | 118 ± 0.1 |
| Ketoconazole (2.7–270 µM)a | 22 ± 0.1a | 18 ± 0.1a |
| Methadone (7.2–720 µM)a | 166 ± 4a | 138 ± 1a |
| Morphine (10–1000 µM) | 6259 ± 103 | 10629 ± 887 |
| Valproic acid (100–7500 µM) | 3575 ± 32 | 3200 ± 19 |
| Zidovudine (10–1000 µM) | 6471 ± 39 | 12818 ± 25 |
↵a IC50 value is the unbound concentration (corrected for nonspecific binding to HLM).