Comparative Pharmacology
Head-to-head clinical analysis: INVEGA TRINZA versus RISPERDAL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: INVEGA TRINZA versus RISPERDAL.
INVEGA TRINZA vs RISPERDAL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Paliperidone is the major active metabolite of risperidone. It is a benzisoxazole derivative antipsychotic that antagonizes central dopamine type 2 (D2) and serotonin type 2 (5-HT2A) receptors. It also antagonizes alpha-1 and alpha-2 adrenergic, and histamine 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.
Administered intramuscularly (gluteal or deltoid) at 3-month intervals. Starting dose: 350 mg, 525 mg, or 700 mg based on prior stabilization dose of oral paliperidone or INVEGA SUSTENNA. Maximum dose: 700 mg.
2-8 mg orally once daily or divided twice daily; maximum 16 mg/day
None Documented
None Documented
Terminal elimination half-life: 3 to 6 months (mean 118 days) due to slow dissolution from intramuscular depot; clinical context: steady state reached after 3 injections every 3 months.
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: 59-80% as unchanged drug and metabolites; fecal: 6-15%; biliary: minimal.
Renal: 70% (30% as unchanged drug, 40% as metabolites), Fecal/Biliary: 14%
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic