Comparative Pharmacology
Head-to-head clinical analysis: ARIPIPRAZOLE versus ZYPREXA RELPREVV.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARIPIPRAZOLE versus ZYPREXA RELPREVV.
ARIPIPRAZOLE vs ZYPREXA RELPREVV
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Partial agonist at D2 and 5-HT1A receptors; antagonist at 5-HT2A receptors.
Olanzapine pamoate is a second-generation antipsychotic that antagonizes dopamine D2 and serotonin 5-HT2A receptors. It also binds to adrenergic α1, histamine H1, and muscarinic M1 receptors.
Oral: 10-15 mg once daily; initial and target dose 10-15 mg; maximum 30 mg/day. IM: 9.75 mg single dose, then 5.25-9.75 mg every 2 hours if needed; maximum 30 mg/day.
210 mg intramuscular injection every 2 weeks; range 150-300 mg; max 300 mg per dose. For olanzapine-naive patients, establish tolerability with oral olanzapine before initiation.
None Documented
None Documented
Aripiprazole has a terminal elimination half-life of approximately 75 hours in extensive CYP2D6 metabolizers and about 146 hours in poor metabolizers. The active metabolite, dehydro-aripiprazole, has a half-life of about 94 hours. This long half-life allows for once-daily dosing and gradual achievement of steady state (14 days in extensive metabolizers).
Clinical Note
moderateAripiprazole + Torasemide
"Aripiprazole may increase the hypotensive activities of Torasemide."
Clinical Note
moderateAripiprazole + Etacrynic acid
"Aripiprazole may increase the hypotensive activities of Etacrynic acid."
Clinical Note
moderateAripiprazole + Furosemide
"Aripiprazole may increase the hypotensive activities of Furosemide."
Clinical Note
moderateAripiprazole + Bumetanide
"Aripiprazole may increase the hypotensive activities of Bumetanide."
The terminal elimination half-life ranges from 30 to 60 days (mean ~45 days) after intramuscular injection, consistent with extended release from the depot formulation.
Aripiprazole is extensively metabolized primarily by the liver via CYP2D6 and CYP3A4. Approximately 25% of the dose is excreted unchanged in urine, and about 55% in feces. The major metabolite, dehydro-aripiprazole, accounts for about 40% of the AUC and is also excreted in urine and feces.
Approximately 57% of the dose is excreted in urine (30% as unchanged drug, 27% as metabolites) and 30% in feces (primarily as metabolites).
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic