Comparative Pharmacology
Head-to-head clinical analysis: PALIPERIDONE PALMITATE versus REXULTI.
Peer-Reviewed Evidence
Head-to-head clinical analysis: PALIPERIDONE PALMITATE versus REXULTI.
PALIPERIDONE PALMITATE vs REXULTI
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Paliperidone is an atypical antipsychotic with high affinity for serotonin 5-HT2A and dopamine D2 receptors. It also blocks alpha-2 adrenergic and H1 histaminergic receptors.
Partial agonist at D2 and 5-HT1A receptors; antagonist at 5-HT2A and α1B/α2C adrenergic receptors.
Paliperidone palmitate is administered intramuscularly. Initial dose: 150 mg eq. on day 1 and 100 mg eq. on day 8, both in the deltoid muscle. Maintenance dose: 75 mg eq. monthly (range 25–150 mg eq.) administered in the deltoid or gluteal muscle.
2 mg orally once daily initially; increase to 4 mg once daily no sooner than week 2; target dose 4 mg once daily; range 2-4 mg once daily.
None Documented
None Documented
Terminal elimination half-life: 25-49 days (mean ~30 days) for IM injection; allows monthly dosing
Terminal elimination half-life is approximately 19–23 days for brexpiprazole and its major metabolite DM-3411, requiring up to 2–3 months to reach steady state.
Renal: 80% as unchanged drug and metabolites; fecal: 11%
Approximately 25% of the dose is excreted in urine as unchanged drug and metabolites; about 54% is excreted in feces. Renal excretion of unchanged drug is minor (<1%).
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic