Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA versus PALIPERIDONE PALMITATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA versus PALIPERIDONE PALMITATE.
ARISTADA vs PALIPERIDONE PALMITATE
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.
Paliperidone is an atypical antipsychotic with high affinity for serotonin 5-HT2A and dopamine D2 receptors. It also blocks alpha-2 adrenergic and H1 histaminergic 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.
Paliperidone palmitate is administered intramuscularly. Initial dose: 150 mg eq. on day 1 and 100 mg eq. on day 8, both in the deltoid muscle. Maintenance dose: 75 mg eq. monthly (range 25–150 mg eq.) administered in the deltoid or gluteal muscle.
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: 25-49 days (mean ~30 days) for IM injection; allows monthly dosing
Primarily renally excreted (approximately 60% as metabolites, <1% unchanged). Fecal elimination accounts for about 20%.
Renal: 80% as unchanged drug and metabolites; fecal: 11%
Category C
Category A/B
Atypical Antipsychotic
Atypical Antipsychotic