Comparative Pharmacology
Head-to-head clinical analysis: INVEGA versus PALIPERIDONE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: INVEGA versus PALIPERIDONE.
INVEGA vs PALIPERIDONE
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 with high affinity for serotonin 5-HT2A and dopamine D2 receptors. It also acts as an antagonist at α1 and α2 adrenergic receptors and H1 histaminergic receptors. It has no affinity for muscarinic 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.
Oral: 6 mg once daily; may increase to 9 mg/day if needed. IM (extended-release): 234 mg on day 1, 156 mg on day 8, then 117 mg monthly; adjust within range 39-234 mg per month.
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 is approximately 23-29 hours for oral administration (paliperidone extended-release). Once-daily dosing achieves steady-state within 4-5 days.
Approximately 23 hours for the extended-release oral formulation; provides steady trough concentrations with once-daily dosing
Primarily renal: 59-80% of dose excreted unchanged in urine (as parent drug and metabolites). Fecal: ~20-30%. Biliary elimination is minimal.
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."