Comparative Pharmacology
Head-to-head clinical analysis: INVEGA SUSTENNA versus PALIPERIDONE.
Head-to-head clinical analysis: INVEGA SUSTENNA versus PALIPERIDONE.
INVEGA SUSTENNA vs PALIPERIDONE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Paliperidone is an atypical antipsychotic that acts primarily as a central dopamine type 2 (D2) receptor antagonist and serotonin type 2A (5-HT2A) receptor antagonist. It also blocks α1- and α2-adrenergic receptors and H1 histamine receptors.
Paliperidone is an atypical antipsychotic that exerts its effects primarily through antagonism of central dopamine D2 receptors and serotonin 5-HT2A receptors. It also antagonizes alpha-1 and alpha-2 adrenergic receptors, and H1 histaminergic receptors. Paliperidone is the major active metabolite of risperidone.
Initiate with 234 mg intramuscular injection on day 1, then 156 mg on day 8, both deltoid. Maintenance: 117 mg monthly (range 39-234 mg) via deltoid or gluteal injection. Dosing based on paliperidone palmitate.
6 mg orally once daily, with dose adjustments in 3 mg increments at intervals of 5 days or more; usual effective range 3-12 mg/day.
None Documented
None Documented
Clinical Note
moderatePaliperidone + Levofloxacin
"Paliperidone may increase the QTc-prolonging activities of Levofloxacin."
Clinical Note
moderatePaliperidone + Norfloxacin
"Paliperidone may increase the QTc-prolonging activities of Norfloxacin."
Clinical Note
moderatePaliperidone + Gemifloxacin
"Paliperidone may increase the QTc-prolonging activities of Gemifloxacin."
Clinical Note
moderatePaliperidone + Fluticasone propionate
Terminal elimination half-life ranges from 25 to 49 days (mean ~38 days) for deltoid injection and 30 to 50 days (mean ~45 days) for gluteal injection, supporting monthly dosing.
Approximately 23 hours for the extended-release oral formulation; provides steady trough concentrations with once-daily dosing
Renal: approximately 59-80% as unchanged drug and metabolites, with about 1% unchanged; biliary/fecal: approximately 20-41% primarily as metabolites.
Renal (approximately 80% as unchanged drug and glucuronide conjugate), biliary/fecal (approximately 11%)
Category C
Category A/B
Atypical Antipsychotic
Atypical Antipsychotic
"The risk or severity of adverse effects can be increased when Paliperidone is combined with Fluticasone propionate."