Comparative Pharmacology
Head-to-head clinical analysis: PALIPERIDONE PALMITATE versus RISPERDAL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: PALIPERIDONE PALMITATE versus RISPERDAL.
PALIPERIDONE PALMITATE vs RISPERDAL
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.
Risperidone is a benzisoxazole atypical antipsychotic that antagonizes dopamine D2 and serotonin 5-HT2A receptors. It also blocks alpha1-adrenergic, alpha2-adrenergic, and histamine H1 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.
2-8 mg orally once daily or divided twice daily; maximum 16 mg/day
None Documented
None Documented
Terminal elimination half-life: 25-49 days (mean ~30 days) for IM injection; allows monthly dosing
20 hours (parent drug), 23 hours (active metabolite 9-hydroxyrisperidone). Steady state reached in 5-6 days. Extended in elderly and hepatic/renal impairment.
Renal: 80% as unchanged drug and metabolites; fecal: 11%
Renal: 70% (30% as unchanged drug, 40% as metabolites), Fecal/Biliary: 14%
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic