Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA versus RISPERDAL CONSTA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA versus RISPERDAL CONSTA.
ARISTADA vs RISPERDAL CONSTA
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.
Risperidone is an atypical antipsychotic with high affinity for serotonin 5-HT2A and dopamine D2 receptors. It also binds to alpha1-adrenergic, alpha2-adrenergic, and histamine H1 receptors, with low affinity for muscarinic receptors. The combination of 5-HT2A and D2 antagonism is thought to improve negative symptoms and reduce extrapyramidal side effects.
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.
25 mg intramuscular every 2 weeks; may increase to 37.5 mg or 50 mg after 4 weeks if needed.
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.
The terminal elimination half-life of risperidone is approximately 20 hours for CYP2D6 extensive metabolizers and 24 hours for poor metabolizers (accounting for both risperidone and 9-hydroxyrisperidone). The half-life of the active moiety is about 20 hours, allowing for biweekly dosing of the long-acting injection.
Primarily renally excreted (approximately 60% as metabolites, <1% unchanged). Fecal elimination accounts for about 20%.
Risperidone and its active metabolite 9-hydroxyrisperidone are primarily excreted renally (70%), with 14% excreted in feces. The remainder is eliminated via biliary and metabolic pathways.
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic