Iloperidone
FANAPT
What it isD2 and 5-HT2A antagonist antipsychotic; schizophrenia and bipolar mania.
Why it mattersAkathisia and extrapyramidal effects are relatively uncommon.
What it changesSlow titration is required because of orthostatic hypotension, making it poor for acute agitation. QT prolongation; CYP2D6-dependent.
FDA-approved for
- schizophrenia (2009)
- bipolar mania (2024)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Schizophrenia | Adults | 1 mg BID | 6–12 mg BID | 12 mg BID |
| Schizophrenia — CYP2D6 poor metabolizers | Adults | 1 mg BID | 3–6 mg BID | 6 mg BID |
Titration Increase daily per schedule over 7 days to target (to limit orthostatic hypotension)
Renal Undefined
Hepatic Mild (Child-Pugh A): no adjustment; moderate (B): may require dose reduction; severe (C): not recommended
Reinitiate titration if treatment interrupted >3 days
Instructions
- Take orally BID with or without food
- Reduce dose by one-half for CYP2D6 poor metabolizers and with strong CYP2D6 and/or CYP3A4 inhibitors
- If off drug >3 days, reinitiate with the initial titration schedule
Cautions
- QT prolongation — avoid with other QT-prolonging drugs
- Cerebrovascular reactions in elderly with dementia
- Neuroleptic malignant syndrome
- Tardive dyskinesia
- Metabolic changes (hyperglycemia, dyslipidemia, weight gain)
- Orthostatic hypotension/syncope
- Seizures
- Leukopenia/neutropenia/agranulocytosis
- Priapism
- Hyperprolactinemia
Adverse reactions
- Dizziness
- Dry mouth
- Fatigue
- Nasal congestion
- Orthostatic hypotension
- Somnolence
- Tachycardia
- Weight increased
Pregnancy Third-trimester exposure risks extrapyramidal and/or withdrawal symptoms in neonates
Lactation Do not breastfeed during treatment
⚠ BOXED WARNING
- Increased mortality in elderly patients with dementia-related psychosis
Cost, est. cash$300–$2,500/month
Generic entry2016
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityMetabolic effects, extrapyramidal symptoms/tardive dyskinesia and agent-specific QT or orthostatic risk.
Active metabolites
Mechanism of action: Iloperidone ballicule
Open Iloperidone in the interactive console ↗
Memory aids: mascots and interaction avatars
Antipsychotics are represented with spooky mascots
Polka dots on pink → α1 blocker → syncope if titrated too quickly (hit the floor)
The fan is napping (unplugged), not restless → low akathisia
