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Atypical Antipsychotic Pharmacokinetics
| ATYPICAL ANTIPSYCHOTIC PHARMACOKINETICS | |||||
|---|---|---|---|---|---|
| Generic | Brand | Form | Bioavailability | Half-life | Cytochrome P450 Metabolism |
| aripiprazole | Abilify | tabs | 87% | ~75hrs (aripiprazole) and ~94hrs (dehydro-aripiprazole) PM: ~146hrs |
CYP 2D6, 3A4 |
| Abilify Mycite | tabs | ||||
| Abilify Maintena | ext-rel inj | — | 30−47 days | ||
| aripiprazole lauroxil | Aristada | ext-rel inj | — | 54–57 days | CYP 2D6, 3A4 |
| Aristada Initio | ext-rel inj | — | 15–18 days (mean) | CYP 3A4, 2D6 | |
| asenapine | Saphris | SL tabs | 35% (absolute) | ~24hrs (mean) | CYP 1A2, 2D6, 3A4 |
| Secuado | transdermal system | — | 30hrs | CYP 1A2 | |
| brexpiprazole | Rexulti | tabs | 95% (absolute) | 91hrs (brexpiprazole) 86hrs (DM3411) |
CYP 2D6, 3A4 |
| cariprazine | Vraylar | caps | — | 2–4 days (cariprazine) 1–3 wks (DDCAR) |
CYP 2D6, 3A4 |
| clozapine | — | ODT | — | 75mg: 8hrs 100mg twice daily: 12hrs |
CYP 1A2, 2D6, 3A4 |
| Clozaril | tabs | ||||
| Versacloz | oral susp | ||||
| iloperidone | Fanapt | tabs | 96% | EM: 18hrs (iloperidone), 26hrs (P88), and 23hrs (P95) PM: 33hrs (iloperidone), 37hrs (P88), and 31hrs (P95) |
CYP 2D6, 3A4 |
| lumateperone | Caplyta | caps | 4.4% (absolute) | 18hrs | CYP 3A4, 2C8, 1A2 |
| lurasidone HCl | Latuda | tabs | 9–19% | ~18hrs (mean) | CYP 3A4 |
| olanzapine | Zyprexa | tabs | ~60% | 21–54hrs | CYP 1A2, 2D6 |
| Zyprexa IntraMuscular | inj | ||||
| Zyprexa Relprevv | ext-rel inj | 30 days | |||
| Zyprexa Zydis | ODT | 21–54hrs | |||
| paliperidone | Invega | ext-rel tabs | 28% (absolute) | ~23hrs | — |
| Invega Hafyera | ext-rel inj | — | 148–159 days | ||
| Invega Sustenna | ext-rel inj | — | 25–49 days | ||
| Invega Trinza | ext-rel inj | — | 84–95 days (deltoid inj) 118–139 days (gluteal inj) |
||
| pimavanserin | Nuplazid | tabs, caps | — | ~57hrs (pimavanserin) ~200hrs (N-desmethylated metabolite) |
CYP 3A4, 3A5, 2J2, 2D6 |
| quetiapine fumarate | Seroquel | tabs | — | ~6hrs | CYP 3A4 |
| Seroquel XR | ext-rel tabs | ~7hrs (quetiapine), 12hrs (N-desalkyl quetiapine) |
|||
| risperidone | Perseris | ext-rel inj | — | 9–11 days (mean) | CYP 2D6, 3A4 |
| Risperdal | tabs, soln | 70% (absolute) | EM: 3hrs (risperidone), 21hrs (9-hydroxyrisperidone) PM: 20hrs (risperidone), 30hrs (9-hydroxyrisperidone) |
CYP 2D6 | |
| Risperdal Consta | long-acting inj | 3–6 days | |||
| Uzedy | ext-rel inj | — | 14–22 days | ||
| ziprasidone HCl | Geodon | caps | ~60% (with food) | ~7hrs | CYP 1A2, 3A4 |
| ziprasidone mesylate | Geodon for inj | inj | 100% | 2–5hrs | CYP 1A2, 3A4 |
| NOTES | |||||
|
Key: EM = extensive metabolizers; ext-rel = extended-release; IR = immediate-release; ODT = orally-disintegrating tablets; PM = poor metabolizers; SL = sublingual Not an inclusive list of medications. Please see drug monograph at www.eMPR.com and/or contact company for full drug labeling. (Rev. 10/2023) |
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