Comparative Pharmacology
Head-to-head clinical analysis: INVEGA HAFYERA versus RISPERIDONE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: INVEGA HAFYERA versus RISPERIDONE.
INVEGA HAFYERA vs RISPERIDONE
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 an atypical antipsychotic that antagonizes dopamine D2 receptors and serotonin 5-HT2A receptors. It also has moderate affinity for alpha1-adrenergic and H1-histaminergic receptors, and low affinity for muscarinic 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.
Initial 2 mg orally once daily, titrated to target dose of 4-6 mg orally once daily (or divided twice daily); maximum 16 mg/day. Alternatively, long-acting IM injection: 25 mg IM every 2 weeks.
None Documented
None Documented
Clinical Note
moderateRisperidone + Fluticasone propionate
"The risk or severity of adverse effects can be increased when Risperidone is combined with Fluticasone propionate."
Clinical Note
moderateRisperidone + Methylphenidate
"The risk or severity of adverse effects can be increased when Risperidone is combined with Methylphenidate."
Clinical Note
moderateRisperidone + Quinagolide
"The therapeutic efficacy of Quinagolide can be decreased when used in combination with Risperidone."
Clinical Note
moderateTerminal 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.
Risperidone: 3 hours (CYP2D6 extensive metabolizers), 20 hours (poor metabolizers); active metabolite 9-hydroxyrisperidone: 21-30 hours; steady-state reached in 5-6 days
Primarily renal: 59% of paliperidone excreted unchanged in urine; 32% as metabolites; 6-12% fecal. Biliary excretion is minimal.
Renal (70% as metabolites, 14% as parent drug) and fecal (14%)
Category C
Category A/B
Atypical Antipsychotic
Atypical Antipsychotic
Risperidone + Cyclosporine
"The metabolism of Cyclosporine can be decreased when combined with Risperidone."