Table 4

In vivo estimates of the relative efficacy (e PD) and receptor affinity (K PD) for flunitrazepam, midazolam, oxazepam, and clobazam on the basis of the mechanism-based pharmacodynamic model, and the in vitro estimates of benzodiazepine receptor affinity (K i) as determined in a benzodiazepine receptor preparation

BenzodiazepineePDKPDKPD,uKIRatioKPD,u/Ki
ng/ml ng/ml ng/ml
Flunitrazepam121  ± 2.13.27.00.46
Midazolam0.87  ± 0.0343  ± 6.01.64.90.33
Oxazepam0.90  ± 0.04411  ± 4936860.42
Clobazam0.79  ± 0.03782  ± 862423500.69

K PD,u reflects the in vivo receptor affinity based on unbound drug concentrations.