Time to peak plasma level (hours) | Half-life (hours), therapeutic | Protein binding (%) | Volume of distribution (L/kg) | Metabolism | Active metabolite(s) | |
Chlorpromazine | 2 to 4 | 23 to 37 (chlorpromazine) 10 to >40 (active metabolites) | 92 to 97 | 8.4 (steady state) 15.7 (single dose) | CYP1A2 CYP2D6 CYP3A4 UGT glucuronidation | Nor1-chlorpromazine 7-OH-chlorpromazine |
Fluphenazine | 2.8 | 14 to 16 | NR | NR | CYP2D6 | NR |
Haloperidol | 2 to 6 | 14 to 37 | 92 | 52.6 (+/– 14.5) | CYP2D6 CYP3A4 UGT glucuronidation | Pyridinium derivative (potential neurotoxin) |
Loxapine | 1 to 2 | 6 to 8 (loxapine) 12 to 19 (active metabolites) | 97 | NR | CYP1A2 CYP2D6 CYP3A4 UGT glucuronidation | 7-hydroxyloxapine 8-hydroxyloxapine |
Perphenazine | 1 to 4 | 9 to 12 (perphenazine) 10 to 19 (active metabolite) | NR | NR | CYP2D6* CYP3A4 Other CYPs | 7-hydroxyperphenazine |
Pimozide | 6 to 8 | 55 150 (poor metabolizers) | 99 | NR | CYP2D6* CYP3A4 | None |
Thioridazine | 1 to 4 | 4 to 10 (thioridazine) 21 to 25 (active metabolites) | 99 | 1.8 to 6.7 | CYP2C19 CYP2D6* | Mesoridazine Sulforidazine |
Thiothixene | 1 to 2 | 34 | 90 | NR | CYP1A2 | NR |
Trifluoperazine | 1.5 to 6 | 3 to 12 (trifluoperazine) 22 (active metabolites) | NR (highly protein bound) | NR | CYP1A2 UGT glucuronidation | N-desmethyltrifluoperazine 7-hydroxyrifluoperazine |
NR: not reported
* Metabolism subject to genetic polymorphism; prolonged half-life and higher plasma concentrations have been observed compared with normal or extensive metabolizers.