Comparative Pharmacology
Head-to-head clinical analysis: ILOPERIDONE versus INVEGA SUSTENNA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ILOPERIDONE versus INVEGA SUSTENNA.
ILOPERIDONE vs INVEGA SUSTENNA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Iloperidone is an atypical antipsychotic with high affinity for serotonin 5-HT2A and dopamine D2 receptors; also moderate affinity for D3, D4, 5-HT6, 5-HT7, and α1-adrenergic receptors; low affinity for H1, 5-HT1A, and α2-adrenergic receptors; no affinity for M1 muscarinic receptors.
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.
1-2 mg orally twice daily; target dose 6-12 mg/day; maximum 12 mg/day
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.
None Documented
None Documented
Clinical Note
moderateIloperidone + Levofloxacin
"Iloperidone may increase the QTc-prolonging activities of Levofloxacin."
Clinical Note
moderateIloperidone + Norfloxacin
"Iloperidone may increase the QTc-prolonging activities of Norfloxacin."
Clinical Note
moderateIloperidone + Gemifloxacin
"Iloperidone may increase the QTc-prolonging activities of Gemifloxacin."
Clinical Note
moderateIloperidone + Haloperidol
"The metabolism of Haloperidol can be decreased when combined with Iloperidone."
Terminal elimination half-life 18 hours in extensive CYP2D6 metabolizers, 33 hours in poor metabolizers; clinical context: steady-state reached in ~5-7 days.
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.
Primarily hepatic metabolism via CYP3A4 and CYP2D6; approximately 7% excreted unchanged in urine and 18% in feces; total renal elimination of metabolites ~25%, fecal ~60%.
Renal: approximately 59-80% as unchanged drug and metabolites, with about 1% unchanged; biliary/fecal: approximately 20-41% primarily as metabolites.
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic