Comparative Pharmacology
Head-to-head clinical analysis: PALIPERIDONE versus SAPHRIS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: PALIPERIDONE versus SAPHRIS.
PALIPERIDONE vs SAPHRIS
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Asenapine is an atypical antipsychotic with high affinity for serotonin 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 receptors; dopamine D2, D3, and D4 receptors; and alpha2-adrenergic receptors. It also has moderate affinity for histamine H1 and alpha1-adrenergic receptors, and low affinity for muscarinic M1 receptors.
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.
5 mg sublingually twice daily, may increase to 10 mg twice daily based on tolerability and efficacy.
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
Approximately 23 hours for the extended-release oral formulation; provides steady trough concentrations with once-daily dosing
Terminal elimination half-life is 30-40 hours, supporting once-daily dosing.
Renal (approximately 80% as unchanged drug and glucuronide conjugate), biliary/fecal (approximately 11%)
After oral administration, approximately 50% of the dose is excreted in urine (mostly as metabolites, <1% unchanged) and 40% in feces (mostly as metabolites).
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic
"The risk or severity of adverse effects can be increased when Paliperidone is combined with Fluticasone propionate."