Comparative Pharmacology
Head-to-head clinical analysis: INVEGA HAFYERA versus RISPERDAL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: INVEGA HAFYERA versus RISPERDAL.
INVEGA HAFYERA vs RISPERDAL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Paliperidone palmitate is an atypical antipsychotic that antagonizes D2 and 5-HT2A receptors, with additional antagonism at alpha2, alpha1, and H1 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.
INVEGA HAFYERA (paliperidone palmitate) is dosed once weekly via intramuscular injection in the gluteal or deltoid muscle. The recommended starting dose is 1,092 mg (deltoid or gluteal) or 1,560 mg (gluteal only) on treatment day 1 and day 8, both given in the deltoid muscle. Subsequent maintenance doses are administered once monthly. Note: INVEGA HAFYERA is only for once-weekly administration; once-monthly formulations (INVEGA SUSTENNA) are also available.
2-8 mg orally once daily or divided twice daily; maximum 16 mg/day
None Documented
None Documented
Terminal elimination half-life is 25-49 days (mean ~36 days) due to slow dissolution from intramuscular depot. Steady-state reached after 4-5 monthly injections.
20 hours (parent drug), 23 hours (active metabolite 9-hydroxyrisperidone). Steady state reached in 5-6 days. Extended in elderly and hepatic/renal impairment.
Primarily renal: 59% of paliperidone excreted unchanged in urine; 32% as metabolites; 6-12% fecal. Biliary excretion is minimal.
Renal: 70% (30% as unchanged drug, 40% as metabolites), Fecal/Biliary: 14%
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic