Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA INITIO KIT versus UZEDY.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA INITIO KIT versus UZEDY.
ARISTADA INITIO KIT vs UZEDY
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 D2 and serotonin 5-HT1A receptors and antagonist at serotonin 5-HT2A receptors. The active metabolite, aripiprazole, exerts antipsychotic effects through modulation of dopaminergic and serotonergic neurotransmission.
Atypical antipsychotic; antagonist at dopamine D2 and serotonin 5-HT1A/5-HT2A receptors; partial agonist at serotonin 5-HT1A receptors
675 mg intramuscularly once, administered as a single dose on day 1 of treatment, followed by oral aripiprazole or ARISTADA 441 mg, 662 mg, or 882 mg on day 8.
UZEDY (risperidone) extended-release injectable suspension: 75 mg, 100 mg, 150 mg, or 200 mg IM gluteal injection every 2 weeks after a single oral dose of 2 mg risperidone for 2 days; or 25 mg, 50 mg, 75 mg, 100 mg, 125 mg, or 150 mg IM every 4 weeks after oral overlap for 2 days. Oral risperidone may be omitted if patient is stable on oral risperidone 2 mg/day.
None Documented
None Documented
The terminal elimination half-life of aripiprazole following a single intramuscular injection of aripiprazole lauroxil is approximately 15-18 days for the 662 mg dose, with a range of 9.4-28.9 days. Steady state is reached after approximately 4 months of monthly dosing.
Terminal half-life approximately 30 days (range 23–37 days) after subcutaneous injection, supporting monthly dosing.
Aripiprazole lauroxil is metabolized to aripiprazole. The primary route of elimination is hepatic metabolism via CYP3A4 and CYP2D6; approximately 25% of the dose is excreted renally as aripiprazole and metabolites, and about 55% is excreted in feces. The active metabolite dehydro-aripiprazole accounts for about 40% of exposure.
Primarily renal: 80% as metabolites, 1% unchanged. Biliary/fecal: 20%.
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic