Relationship between dose, mode of administration (injection vs. minipump), D2 occupancy, and plasma levels at different doses of antipsychotics with multiple-dose administration
Drug Group | Delivery Condition | D2 Occupancy (Mean ± S.D.) | Plasma Levels (Mean ± S.D.) |
|---|---|---|---|
| nM | |||
| Haloperidol | |||
| 0.05 mg/kg | Injection, trough | 19 ± 31 | <1 |
| Injection, peak | 74 ± 7 | 1.57 ± 0.42 | |
| Minipump | 41 ± 16 | <1 | |
| 0.25 mg/kg | Injection, trough | 5 ± 2 | <1 |
| Injection, peak | 92 ± 1 | 11 ± 2.08 | |
| Minipump | 69 ± 14 | 2.40 ± 1.01 | |
| Olanzapine | |||
| 1.5 mg/kg | Injection, trough | 16 ± 24 | 6.67 + 2.89 |
| Injection, peak | 74 ± 7 | 251 ± 88.39 | |
| Minipump | 38 ± 16 | 130.83 ± 118.90 | |
| 7.5 mg/kg | Injection, trough | 59 ± 4 | <5 |
| Injection, peak | 92 ± 1 | 3124.33 ± 823.29 | |
| Minipump | 75 ± 7 | 434.33 ± 291.19 | |
| Risperidone | |||
| 1 mg/kg | Injection, trough | ND | <1 |
| Injection, peak | 61 ± 3 | 99.97 ± 33.77 | |
| Minipump | 31 ± 9 | 39.36 ± 24.36 | |
| Quetiapine | |||
| 10 mg/kg | Injection, trough | ND | 4.56 ± 2.71 |
| Injection, peak | ND | 469.00 ± 18.96 | |
| Minipump | 7 ± 10 | 108.20 ± 31.88 | |
| 25 mg/kg | Injection, trough | ND | 9.56 ± 7.8 |
| Injection, peak | 69 ± 10 | 913.01 ± 223.5 | |
| Minipump | 25 ± 23 | 78.79 ± 12.33 | |
| Clozapine | |||
| 7.5 mg/kg | Injection, trough | ND | 13 ± 3 |
| Injection, peak | 29 ± 15 | 1240 ± 438.42 | |
| Minipump | 2 ± 22 | 98 ± 128.83 | |
| 15 mg/kg | Injection, trough | 0.2 ± 20 | 15 ± 6.35 |
| Injection, peak | 60 ± 12 | 2969 ± 809.60 | |
|
| Minipump | ND | 98 ± 45.30 |
ND, no detectable occupancy.