Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA versus CLOZAPINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA versus CLOZAPINE.
ARISTADA vs CLOZAPINE
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.
Atypical antipsychotic; binds to dopamine D4, serotonin 5-HT2A, and adrenergic α2 receptors; weak D2 antagonist with rapid dissociation; also affects histaminergic and cholinergic 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: 12.5 mg orally once or twice daily; titrate gradually by 25-50 mg/day to target dose 300-450 mg/day in divided doses; max 900 mg/day.
None Documented
None Documented
Clinical Note
moderateClozapine + Norfloxacin
"Clozapine may increase the QTc-prolonging activities of Norfloxacin."
Clinical Note
moderateClozapine + Torasemide
"The risk or severity of adverse effects can be increased when Clozapine is combined with Torasemide."
Clinical Note
moderateClozapine + Etacrynic acid
"The risk or severity of adverse effects can be increased when Clozapine is combined with Etacrynic acid."
Clinical Note
moderateClozapine + Furosemide
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 8 to 12 hours (steady-state), but can range from 4 to 66 hours; requires dose adjustment in renal/hepatic impairment.
Primarily renally excreted (approximately 60% as metabolites, <1% unchanged). Fecal elimination accounts for about 20%.
Approximately 50% of the dose is excreted in urine (30% as unchanged drug and metabolites) and 30% in feces via biliary elimination.
Category C
Category A/B
Atypical Antipsychotic
Atypical Antipsychotic
"The risk or severity of adverse effects can be increased when Clozapine is combined with Furosemide."