Comparative Pharmacology
Head-to-head clinical analysis: ARISTADA INITIO KIT versus PALIPERIDONE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARISTADA INITIO KIT versus PALIPERIDONE.
ARISTADA INITIO KIT vs PALIPERIDONE
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.
Paliperidone is an atypical antipsychotic that exerts its effects primarily through antagonism of central dopamine D2 receptors and serotonin 5-HT2A receptors. It also antagonizes alpha-1 and alpha-2 adrenergic receptors, and H1 histaminergic receptors. Paliperidone is the major active metabolite of risperidone.
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.
6 mg orally once daily, with dose adjustments in 3 mg increments at intervals of 5 days or more; usual effective range 3-12 mg/day.
None Documented
None Documented
Clinical Note
moderatePaliperidone + Levofloxacin
"Paliperidone may increase the QTc-prolonging activities of Levofloxacin."
Clinical Note
moderatePaliperidone + Norfloxacin
"Paliperidone may increase the QTc-prolonging activities of Norfloxacin."
Clinical Note
moderatePaliperidone + Gemifloxacin
"Paliperidone may increase the QTc-prolonging activities of Gemifloxacin."
Clinical Note
moderatePaliperidone + 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.
Approximately 23 hours for the extended-release oral formulation; provides steady trough concentrations with once-daily 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.
Renal (approximately 80% as unchanged drug and glucuronide conjugate), biliary/fecal (approximately 11%)
Category C
Category A/B
Atypical Antipsychotic
Atypical Antipsychotic
"The risk or severity of adverse effects can be increased when Paliperidone is combined with Fluticasone propionate."