Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA versus NUPLAZID.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA versus NUPLAZID.
ARISTADA vs NUPLAZID
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.
Selective serotonin 5-HT2A receptor inverse agonist and antagonist; also has moderate affinity for 5-HT2C and 5-HT1A 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.
34 mg orally once daily.
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 50 hours (range 40-70 hours), allowing once-daily dosing.
Primarily renally excreted (approximately 60% as metabolites, <1% unchanged). Fecal elimination accounts for about 20%.
Fecal (approximately 60%) as unchanged drug and metabolites; renal (approximately 13%) as unchanged drug and metabolites.
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic