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	CYP 2D6, 3A4
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)	CYP 3A4
risperidone	Risperdal	tabs, soln	70% (absolute)	EM: 3hrs, PM: 20hrs	CYP 2D6
	Risperdal Consta	long-acting inj		3–6 days	CYP 2D6
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)

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