Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA versus INVEGA SUSTENNA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA versus INVEGA SUSTENNA.
ARISTADA vs INVEGA SUSTENNA
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 that acts primarily as a central dopamine type 2 (D2) receptor antagonist and serotonin type 2A (5-HT2A) receptor antagonist. It also blocks α1- and α2-adrenergic receptors and H1 histamine 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.
Initiate with 234 mg intramuscular injection on day 1, then 156 mg on day 8, both deltoid. Maintenance: 117 mg monthly (range 39-234 mg) via deltoid or gluteal injection. Dosing based on paliperidone palmitate.
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 ranges from 25 to 49 days (mean ~38 days) for deltoid injection and 30 to 50 days (mean ~45 days) for gluteal injection, supporting monthly dosing.
Primarily renally excreted (approximately 60% as metabolites, <1% unchanged). Fecal elimination accounts for about 20%.
Renal: approximately 59-80% as unchanged drug and metabolites, with about 1% unchanged; biliary/fecal: approximately 20-41% primarily as metabolites.
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic