Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA versus RISPERIDONE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA versus RISPERIDONE.
ARISTADA vs RISPERIDONE
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 that antagonizes dopamine D2 receptors and serotonin 5-HT2A receptors. It also has moderate affinity for alpha1-adrenergic and H1-histaminergic receptors, and low affinity for muscarinic 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.
Initial 2 mg orally once daily, titrated to target dose of 4-6 mg orally once daily (or divided twice daily); maximum 16 mg/day. Alternatively, long-acting IM injection: 25 mg IM every 2 weeks.
None Documented
None Documented
Clinical Note
moderateRisperidone + Fluticasone propionate
"The risk or severity of adverse effects can be increased when Risperidone is combined with Fluticasone propionate."
Clinical Note
moderateRisperidone + Methylphenidate
"The risk or severity of adverse effects can be increased when Risperidone is combined with Methylphenidate."
Clinical Note
moderateRisperidone + Quinagolide
"The therapeutic efficacy of Quinagolide can be decreased when used in combination with Risperidone."
Clinical Note
moderateTerminal elimination half-life of aripiprazole lauroxil (the prodrug in ARISTADA) is approximately 54 days (range 29-74 days) after IM injection, allowing monthly dosing.
Risperidone: 3 hours (CYP2D6 extensive metabolizers), 20 hours (poor metabolizers); active metabolite 9-hydroxyrisperidone: 21-30 hours; steady-state reached in 5-6 days
Primarily renally excreted (approximately 60% as metabolites, <1% unchanged). Fecal elimination accounts for about 20%.
Renal (70% as metabolites, 14% as parent drug) and fecal (14%)
Category C
Category A/B
Atypical Antipsychotic
Atypical Antipsychotic
Risperidone + Cyclosporine
"The metabolism of Cyclosporine can be decreased when combined with Risperidone."