Table 2.
Treatment group (mg/kg/day) |
Average D2 receptor occupancya |
Average D2 receptor occupancya (peak + trough) |
Average plasma drug levels (ng/ml) |
Average plasma levels (ng/ml) (peak + trough) |
---|---|---|---|---|
Haloperidol: | ||||
1.5 Peak | 85.78 ± 3.69 | 5.02 ± 1.96 | ||
1.5 Trough | 68.43 ± 5.99 | 77.11 ± 10.54 | 1.84 ± 0.53 | 3.43 ± 2.26 |
2.0 Peak | 86.43 ± 4.66 | 3.36 ± 1.58 | ||
2.0 Trough | 70.94 ± 7.43 | 78.68 ± 10.46 | 1.68 ± 0.43 | 2.52 ± 1.51 |
Clozapine: | ||||
20 Peak | 16.07 ± 11.79 | 8.6 ± 1.02 | ||
20 Trough | −13.32 ± 10.85 | 1.37 ± 19.84 | 1.8 ± 3.6 | 5.25 ± 4.40 |
40 Peak | 26.93 ± 18.42 | 29.8 ± 17.27 | ||
40 Trough | −6.33 ± 18.23 | 10.30 ± 26.09 | 6.0 ± 3.10 | 17.9 ± 18.12 |
Olanzapine: | ||||
2 Peak | 32.50 ± 9.26 | 1.54 ± 0.67 | ||
2 Trough | 12.78 ± 11.78 | 22.64 ± 15.47 | 0.16 ± 0.32 | 0.87 ± 0.95 |
4 Peak | 42.20 ± 19.69 | 7.58 ± 4.95 | ||
4 Trough | 36.98 ± 14.59 | 39.88 ± 18.88 | 1.24 ± 1.38 | 4.81 ± 5.22 |
5 Peak | 44.14 ± 13.03 | 8.62 ± 2.87 | ||
5 Trough | 33.44 ± 7.86 | 39.39 ± 12.99 | 0.8 ± 0.26 | 5.13 ± 4.72 |
D2 receptor occupancy values are shown as the percentage of control animals. In human patients clinically relevant receptor occupancy values are 65–80% for haloperidol and olanzapine, and 45–65% for clozapine (Kapur et al. 2003)