Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA INITIO KIT versus SEROQUEL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA INITIO KIT versus SEROQUEL.
ARISTADA INITIO KIT vs SEROQUEL
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.
Antagonist at dopamine D2 and serotonin 5-HT2A receptors; also blocks histamine H1 and adrenergic α1 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.
Initial: 25 mg twice daily; titrate by 25-50 mg twice daily on day 2 and 3 to target 300-400 mg daily in 2-3 divided doses. Maintenance: 400-800 mg daily. Maximum: 800 mg daily.
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 elimination half-life approximately 7 hours for quetiapine; for metabolite N-desalkylquetiapine (norquetiapine), approximately 12 hours. Steady-state reached within 2 days.
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 hepatic metabolism; <1% excreted unchanged renally. Metabolites excreted in urine (73%) and feces (20%).
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic