Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA versus LURASIDONE HYDROCHLORIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA versus LURASIDONE HYDROCHLORIDE.
ARISTADA vs LURASIDONE HYDROCHLORIDE
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.
Lurasidone is an atypical antipsychotic that acts as a full antagonist at D2 and 5-HT2A receptors, with high affinity for 5-HT7 and 5-HT1A receptors, moderate affinity for alpha2C and alpha2A adrenergic receptors, and no appreciable affinity for H1, M1, or alpha1 receptors.
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.
40 mg orally once daily initially, titrated to 80 mg once daily; maximum 80 mg per day.
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 is approximately 18 hours (range 14–24 hours), supporting once-daily dosing.
Primarily renally excreted (approximately 60% as metabolites, <1% unchanged). Fecal elimination accounts for about 20%.
Approximately 80% of total radioactivity recovered in feces (67% as metabolites, 9% as unchanged drug) and 19% in urine (mostly metabolites); less than 1% excreted as unchanged parent in urine.
Category C
Category A/B
Atypical Antipsychotic
Atypical Antipsychotic