Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA versus ZYPREXA ZYDIS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA versus ZYPREXA ZYDIS.
ARISTADA vs ZYPREXA ZYDIS
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Aripiprazole lauroxil is a prodrug of aripiprazole, a partial agonist at dopamine D2 and serotonin 5-HT1A receptors and an antagonist at 5-HT2A receptors. The mechanism of action in schizophrenia and bipolar I disorder is thought to be mediated through these receptor interactions.
Olanzapine is an atypical antipsychotic with high affinity for serotonin 5-HT2A and 5-HT2C receptors, dopamine D1-D4 receptors, muscarinic M1-M5 receptors, histamine H1 receptors, and alpha1-adrenergic receptors. Antagonism at D2 and 5-HT2A receptors is primarily responsible for its antipsychotic effects.
Initial dose: 675 mg intramuscularly every 4 weeks for the first 2 doses, then maintenance dose of 882 mg intramuscularly every 4 weeks. Alternatively, 1064 mg intramuscularly every 6 weeks after appropriate initiation.
10 mg orally once daily; range 5-20 mg once daily. Initial dose 5-10 mg, titrate by 5 mg weekly. Maximum 20 mg/day. Orally disintegrating tablet.
None Documented
None Documented
Terminal elimination half-life of aripiprazole lauroxil (the prodrug in ARISTADA) is approximately 54 days (range 29-74 days) after IM injection, allowing monthly dosing.
Terminal elimination half-life: ~30 hours (range 21–54 hours) in healthy adults; prolonged in elderly (mean 51.8 h) and hepatic impairment.
Primarily renally excreted (approximately 60% as metabolites, <1% unchanged). Fecal elimination accounts for about 20%.
Renal: ~57% (as metabolites); Fecal: ~30% (as metabolites); Unchanged olanzapine in urine <7%.
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic