Comparative Pharmacology
Head-to-head clinical analysis: ILOPERIDONE versus RISPERDAL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ILOPERIDONE versus RISPERDAL.
ILOPERIDONE vs RISPERDAL
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.
Risperidone is a benzisoxazole atypical antipsychotic that antagonizes dopamine D2 and serotonin 5-HT2A receptors. It also blocks alpha1-adrenergic, alpha2-adrenergic, and histamine H1 receptors.
1-2 mg orally twice daily; target dose 6-12 mg/day; maximum 12 mg/day
2-8 mg orally once daily or divided twice daily; maximum 16 mg/day
None Documented
None Documented
Terminal elimination half-life 18 hours in extensive CYP2D6 metabolizers, 33 hours in poor metabolizers; clinical context: steady-state reached in ~5-7 days.
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."
20 hours (parent drug), 23 hours (active metabolite 9-hydroxyrisperidone). Steady state reached in 5-6 days. Extended in elderly and hepatic/renal 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: 70% (30% as unchanged drug, 40% as metabolites), Fecal/Biliary: 14%
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic