Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA versus QUETIAPINE FUMARATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA versus QUETIAPINE FUMARATE.
ARISTADA vs QUETIAPINE FUMARATE
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.
Antagonist at serotonin 5-HT2A, dopamine D2, histamine H1, alpha1-adrenergic, and muscarinic M1 receptors. Also partial agonist at serotonin 5-HT1A and dopamine D2 receptors (depending on dose).
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.
Immediate release: 25-100 mg orally twice daily, titrated as needed up to 400-800 mg/day divided twice daily. Extended release: 50-200 mg orally once daily, titrated up to 400-800 mg/day 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 6-7 hours (quetiapine) and 9-12 hours for the active metabolite norquetiapine; with extended-release formulation, effective half-life is ~7 hours due to slower absorption. Clinical steady-state achieved within 2 days.
Primarily renally excreted (approximately 60% as metabolites, <1% unchanged). Fecal elimination accounts for about 20%.
Renal: 73% (20% unchanged, remainder as metabolites); Fecal: 21%; Approximately 5% excreted in feces as unchanged drug.
Category C
Category A/B
Atypical Antipsychotic
Atypical Antipsychotic