Comparative Pharmacology
Head-to-head clinical analysis: PALIPERIDONE PALMITATE versus UZEDY.
Peer-Reviewed Evidence
Head-to-head clinical analysis: PALIPERIDONE PALMITATE versus UZEDY.
PALIPERIDONE PALMITATE vs UZEDY
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.
Atypical antipsychotic; antagonist at dopamine D2 and serotonin 5-HT1A/5-HT2A receptors; partial agonist at serotonin 5-HT1A 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.
UZEDY (risperidone) extended-release injectable suspension: 75 mg, 100 mg, 150 mg, or 200 mg IM gluteal injection every 2 weeks after a single oral dose of 2 mg risperidone for 2 days; or 25 mg, 50 mg, 75 mg, 100 mg, 125 mg, or 150 mg IM every 4 weeks after oral overlap for 2 days. Oral risperidone may be omitted if patient is stable on oral risperidone 2 mg/day.
None Documented
None Documented
Terminal elimination half-life: 25-49 days (mean ~30 days) for IM injection; allows monthly dosing
Terminal half-life approximately 30 days (range 23–37 days) after subcutaneous injection, supporting monthly dosing.
Renal: 80% as unchanged drug and metabolites; fecal: 11%
Primarily renal: 80% as metabolites, 1% unchanged. Biliary/fecal: 20%.
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic