Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA INITIO KIT versus LATUDA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA INITIO KIT versus LATUDA.
ARISTADA INITIO KIT vs LATUDA
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.
Lurasidone is an atypical antipsychotic with high affinity for dopamine D2, serotonin 5-HT2A, and serotonin 5-HT7 receptors, and moderate affinity for serotonin 5-HT1A receptors. It acts as an antagonist at D2 and 5-HT2A receptors, and as a partial agonist at 5-HT1A receptors. The exact mechanism of action in schizophrenia and bipolar depression is unknown but is thought to involve modulation of these 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.
40 mg orally once daily initially, titrated to 80-160 mg once daily; maximum 160 mg/day. Administer with food (at least 350 calories).
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 is approximately 20–40 hours (mean about 29 hours) in adults, supporting once-daily dosing. Steady-state is reached within 7 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.
Approximately 80% of the dose is eliminated in feces (mostly as unchanged drug and metabolites) and about 10% in urine. Less than 2% is excreted as unchanged lurasidone in urine.
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic