Time to therapeutic peak plasma level (hours) | Half-life (hours), therapeutic | Protein binding (%) | Volume of distribution (L/kg) | Major route(s) of metabolism | Active metabolite(s) | |
Aripiprazole | 3 to 5 | 74 (aripiprazole) 94 (active metabolite) 146 (poor metabolizers) | >99 | 4.9 | CYP2D6 CYP3A4 | Dehydroaripiprazole |
Asenapine | 0.5 to 1.5 (SL) 12 to 24 (TD) | 24 (SL) 30 (TD) | 95 | 20 to 25 | CYP1A2 UGT1A4 glucuronidation | None |
Brexpiprazole | 4 | 91 | >99 | 1.6 | CYP2D6 CYP3A4 | None |
Cariprazine | 3 to 6 | 2 to 4 days (cariprazine) 1 to 21 days (active metabolites) | 91 to 97 | NR | CYP3A4 | Desmethyl cariprazine Didesmethyl cariprazine |
Clozapine | 1 to 6 | 7 to 13 | 97 | 2 to 5 | CYP1A2 CYP3A4 | N-desmethylclozapine (limited activity) |
Iloperidone | 2 to 4 | 18 (iloperidone) 23 to 26 (active metabolites) 31 to 37 (poor metabolizers) | 97 | 17 to 35 | CYP2D6 CYP3A4 | P88 P95 |
Lumateperone | 1 to 2 | 18 | 97 | 4.1 | CYP3A4 UGT 1A1,1A4, 2B15 glucuronidation | IC200161 |
Lurasidone | 1 to 3 | 18 to 40 (Lurasidone) 7.5 to 10 (active metabolites) | 99 | 77 | CYP3A4 | ID-14283 ID-14326 |
Olanzapine | 5 to 6 | 30 (21 to 54) | 93 | 10 to 20 | CYP1A2 UGT1A4 glucuronidation | None |
Paliperidone | 24 | 23 24 to 51 (kidney impairment) | 74 | NR | Minimal hepatic metabolism; excreted mainly unchanged in urine | None |
Pimavanserin | 6 | 57 (pimavanserin) 200 (active metabolite) | 95 | 27 | CYP3A4/5 | AC-279 |
Quetiapine | 1 to 2 (IR) 6 (ER) | 4 to 10 (quetiapine) 12 (active metabolite) | 83 | 10 | CYP3A4 | N-desalkyl quetiapine |
Risperidone | 1 to 2 | 3 (risperidone) 21 (active metabolite) 20 to 30 (poor metabolizers) | 90 (risperidone) 77 (active metabolite) | 1 to 2 | CYP2D6 CYP3A4 Substrate of P-glycoprotein efflux | 9-hydroxyrisperidone |
Ziprasidone | 6 to 8 | 7 (4 to 10) | >99 | 1.5 | CYP3A4 | None |