Kinetic parameters for inhibition of midazolam hydroxylation by macrolides
Erythromycin | Clarithromycin | Azithromycin | |||||||
|---|---|---|---|---|---|---|---|---|---|
|
α-OH
|
4-OH
|
α-OH
|
4-OH
|
α-OH
|
4-OH
| ||||
| K′app (μM) | 12.6 | 14.1 | 41.4 | 37.0 | 623 | 690 | |||
| kinact (min-1) | 0.0240 | 0.0256 | 0.0423 | 0.0459 | 0.0158 | 0.0248 | |||
| kd (min-1)
|
0.0030
|
0.0039
|
0.0036
|
0.0048
|
0.0025
|
0.0033
| |||