Iloperidone

FANAPT

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Pronunciation: eye-loe-PER-i-doen

Iloperidone ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Iloperidone ballicule

Iloperidone FANAPT mascot mnemonic cartoon — Visual mnemonic: Iloperidone mascot
**“Fan napped (with) Eye opener”**
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

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.

Iloperidone molecular structure (skeletal formula) — Molecular structure: Iloperidone

FDA-approved for

schizophrenia (2009)
bipolar mania (2024)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Increased mortality in elderly patients with dementia-related psychosis.

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

Available strengths

tab 1, 2, 4, 6, 8, 10, 12 mg

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

Cost

Iloperidone (FANAPT)

What pharmacies pay · NADAC 9/30/26

Strength		#/mo	generic $/mo	brand $/mo	CostPlus
1 mg	tab	60 BID	—	$1,829.91	not offered
2 mg	tab	60 BID	—	$1,844.26	not offered
4 mg	tab	60 BID	—	$1,831.81	not offered
6 mg	tab	60 BID	—	$2,256.86	not offered
8 mg	tab	60 BID	—	$2,248.94	not offered
10 mg	tab	60 BID	—	$3,617.19	not offered
12 mg	tab	60 BID	—	$3,600.60	not offered

Generic entry2016

⚠ BOXED WARNING

Increased mortality in elderly patients with dementia-related psychosis

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger2 / 4

Weight-gain liability2 / 4

Sedation liability2 / 4

QT / Torsades1 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityMetabolic effects, extrapyramidal symptoms/tardive dyskinesia and agent-specific QT or orthostatic risk.

Active metabolites

Milsaperidone

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Memory aids: interaction avatars

CYP2D6 substrate

CYP3A4 substrate

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