Comparative Pharmacology
Head-to-head clinical analysis: ILOPERIDONE versus INVEGA TRINZA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ILOPERIDONE versus INVEGA TRINZA.
ILOPERIDONE vs INVEGA TRINZA
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 the major active metabolite of risperidone. It is a benzisoxazole derivative antipsychotic that antagonizes central dopamine type 2 (D2) and serotonin type 2 (5-HT2A) receptors. It also antagonizes alpha-1 and alpha-2 adrenergic, and histamine H1 receptors.
1-2 mg orally twice daily; target dose 6-12 mg/day; maximum 12 mg/day
Administered intramuscularly (gluteal or deltoid) at 3-month intervals. Starting dose: 350 mg, 525 mg, or 700 mg based on prior stabilization dose of oral paliperidone or INVEGA SUSTENNA. Maximum dose: 700 mg.
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: 3 to 6 months (mean 118 days) due to slow dissolution from intramuscular depot; clinical context: steady state reached after 3 injections every 3 months.
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: 59-80% as unchanged drug and metabolites; fecal: 6-15%; biliary: minimal.
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic