Comparative Pharmacology
Head-to-head clinical analysis: LUMATEPERONE TOSYLATE versus PALIPERIDONE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LUMATEPERONE TOSYLATE versus PALIPERIDONE.
LUMATEPERONE TOSYLATE vs PALIPERIDONE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Lumateperone tosylate is an atypical antipsychotic with a unique mechanism of action involving antagonism of serotonin 5-HT2A receptors, partial agonism of serotonin 5-HT1A receptors, and antagonism of dopamine D2 receptors; it also modulates glutamate via phosphorylation of GluN2B subunits and inhibits serotonin reuptake.
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.
42 mg orally once daily
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 24-29 hours, allowing once-daily dosing. Steady-state reached in about 5 days.
Approximately 23 hours for the extended-release oral formulation; provides steady trough concentrations with once-daily dosing
Approximately 60% excreted in urine as metabolites (unchanged drug negligible) and 30% in feces via biliary elimination.
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."