Second-generation (atypical) antipsychotic
Antagonist at dopamine D2 and serotonin 5-HT2A receptors, with additional antagonism at alpha-1 adrenergic receptors contributing to orthostatic hypotension risk; moderate affinity for histamine H1 and muscarinic receptors
Schizophrenia
Augmentation in bipolar disorder, management of psychosis in neuropsychiatric populations prioritizing metabolic tolerability
Oral tablets
Start at 1 mg orally twice daily, titrated slowly over 4–7 days to minimize orthostatic hypotension risk
12–24 mg/day divided BID
Extensive hepatic metabolism via CYP2D6 and CYP3A4; half-life approximately 18 hours; steady state reached in 3–4 days
Dizziness, orthostatic hypotension, sedation, dry mouth, weight gain
QT prolongation; caution in patients with cardiac risk factors
Baseline and periodic blood pressure monitoring to detect orthostatic hypotension; ECG recommended for patients with cardiac risk or symptoms; monitor weight and metabolic parameters periodically
Increased mortality in elderly patients with dementia-related psychosis
Iloperidone may have a more favorable metabolic profile than other second generation (atypical) antipsychotic agents, but is limited by the need for slow titration and QT prolongation risk. Use caution in elderly patients, those with autonomic instability, and patients with poor adherence due to BID dosing requirements.