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 Maintena ext-rel inj 30−47 days
aripiprazole lauroxil Aristada ext-rel inj 54–57 days CYP 2D6, 3A4
asenapine Saphris SL tabs 35% (absolute) ~24hrs (mean) CYP 1A2, 2D6, 3A4
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 Clozaril tabs 75mg: 8hrs
100mg twice daily: 12hrs
CYP 1A2, 2D6, 3A4
Fazaclo ODT
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
lurasidone HCl Latuda tabs 9–19% ~18hrs (mean) CYP 3A4
olanzapine Zyprexa tabs ~60% 21–54hrs CYP 1A2, 2D6
Zyprexa Zydis ODT
Zyprexa IntraMuscular inj
paliperidone Invega ext-rel tabs 28% (absolute) ~23hrs
Invega Sustenna ext-rel inj 25–49 days
Invega Trinza ext-rel inj 84–95 days (deltoid inj)
118–139 days (gluteal inj)
quetiapine fumarate Seroquel tabs ~6hrs CYP 3A4
Seroquel XR ext-rel tabs ~7hrs (quetiapine),
12hrs (N-desalkyl quetiapine)
risperidone Risperdal tabs, soln 70% (absolute) EM: 3hrs, PM: 20hrs CYP 2D6
Risperdal Consta long-acting inj 3–6 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. 1/2018)

This article originally appeared on MPR