Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA INITIO KIT versus QUETIAPINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA INITIO KIT versus QUETIAPINE.
ARISTADA INITIO KIT vs Quetiapine
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 serotonin 5-HT2A, dopamine D2, histamine H1, and adrenergic α1 receptors; weak partial agonist at 5-HT1A and serotonin transporter.
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 PO BID, titrate to effective range 150-750 mg/day divided BID-TID; schizophrenia: 150-750 mg/day, bipolar disorder: 400-800 mg/day, major depressive disorder (adjunct): 150-300 mg/day at bedtime.
None Documented
None Documented
Clinical Note
moderateQuetiapine + Levofloxacin
"Quetiapine may increase the QTc-prolonging activities of Levofloxacin."
Clinical Note
moderateQuetiapine + Norfloxacin
"Quetiapine may increase the QTc-prolonging activities of Norfloxacin."
Clinical Note
moderateQuetiapine + Gemifloxacin
"Quetiapine may increase the QTc-prolonging activities of Gemifloxacin."
Clinical Note
moderateQuetiapine + Fluticasone propionate
"The risk or severity of adverse effects can be increased when Quetiapine is combined with Fluticasone propionate."
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: ~6-7 hours (parent drug); extended-release: ~7 hours. Clinically, dosing is twice daily for immediate-release; once daily for extended-release.
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.
Renal: 73% (as metabolites), Fecal: 20% (as metabolites), unchanged drug: <1% renal
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic