Comparative Pharmacology
Head-to-head clinical analysis: ILOPERIDONE versus ZYPREXA ZYDIS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ILOPERIDONE versus ZYPREXA ZYDIS.
ILOPERIDONE vs ZYPREXA ZYDIS
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.
Olanzapine is an atypical antipsychotic with high affinity for serotonin 5-HT2A and 5-HT2C receptors, dopamine D1-D4 receptors, muscarinic M1-M5 receptors, histamine H1 receptors, and alpha1-adrenergic receptors. Antagonism at D2 and 5-HT2A receptors is primarily responsible for its antipsychotic effects.
1-2 mg orally twice daily; target dose 6-12 mg/day; maximum 12 mg/day
10 mg orally once daily; range 5-20 mg once daily. Initial dose 5-10 mg, titrate by 5 mg weekly. Maximum 20 mg/day. Orally disintegrating tablet.
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: ~30 hours (range 21–54 hours) in healthy adults; prolonged in elderly (mean 51.8 h) and hepatic impairment.
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: ~57% (as metabolites); Fecal: ~30% (as metabolites); Unchanged olanzapine in urine <7%.
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic