iloperidone

Antipsychotic

Brands: Fanapt

Last reviewed 2025-09-26

Reviewed by PsychMed Editorial Team.

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Quick answers

What is iloperidone?
Iloperidone (brand Fanapt) is a second-generation antipsychotic approved in 2009 for adult schizophrenia and is often considered when patients need a lower-EPS option.
What is Fanapt?
Fanapt is a brand name for iloperidone.
What is Fanapt (iloperidone) used for?
Label indications include: Schizophrenia (adults).
What drug class is Fanapt (iloperidone)?
Antipsychotic.
What is the mechanism of action of Fanapt (iloperidone)?
Dopamine D2/D3 and serotonin 5-HT2A antagonist with high affinity for adrenergic α1 receptors, requiring slow titration.
What strengths does Fanapt (iloperidone) come in?
Tablets: 1 mg, 2 mg, 4 mg, 6 mg, 8 mg, 10 mg, 12 mg.
Is Fanapt (iloperidone) a controlled substance?
No — it is not scheduled as a controlled substance under U.S. federal law.

Snapshot

Class: Antipsychotic
Common US brands: Fanapt
Therapeutic drug monitoring not routinely recommended.
Last reviewed: 2025-09-26

Clinical Highlights

Iloperidone (brand Fanapt) is a second-generation antipsychotic approved in 2009 for adult schizophrenia and is often considered when patients need a lower-EPS option. Potent antagonism at adrenergic α1 receptors necessitates a structured titration schedule to mitigate orthostatic hypotension, syncope, and tachycardia.

Tablet strengths from 1 mg to 12 mg enable fine-tuned dosing; therapy must restart at 1 mg twice daily if treatment is interrupted for three or more consecutive days.
Use is tempered by slow titration and QTc warnings, yet iloperidone can be useful when other SGAs cause EPS or metabolic burden.
Schizophrenia (adults) (FDA 2009)
Generic: Generic tablets available in the U.S. market.
The compare tool and the evidence library, together with the Schizophrenia hub, support side-by-side review of low-EPS alternatives and follow-up planning.

Dosing & Formulations

Tablets: 1 mg, 2 mg, 4 mg, 6 mg, 8 mg, 10 mg, 12 mg. Titrate: Day 1 1 mg BID → Day 2 2 mg BID → Day 3 4 mg BID → Day 4 6 mg BID → Day 5 8 mg BID; maintenance target 6–12 mg BID (12–24 mg/day).

Target and maximum doses are typically reduced by 50% in CYP2D6 poor metabolizers or when co-administered with strong CYP2D6 inhibitors (fluoxetine, paroxetine).
Dose reductions (often ~50%) are commonly used with strong CYP3A4 inhibitors (ketoconazole, clarithromycin), with attention to QTc. Strong CYP3A4 inducers (carbamazepine, rifampin) can markedly reduce exposure and are generally avoided.
If therapy is interrupted for ≥3 consecutive days, titration is typically restarted at 1 mg twice daily to reduce orthostatic events.

Monitoring & Risks

Boxed warning: Antipsychotics increase mortality in elderly patients with dementia-related psychosis; iloperidone is not approved for this population. Orthostatic hypotension/syncope: Most pronounced during titration; counseling often includes hydration and slow position changes.

Tachycardia and palpitations: Pulse is often monitored, particularly with concomitant QTc-prolonging drugs.
Somnolence and dizziness: May improve after the first week; some dosing strategies shift a larger portion to bedtime when tolerated.
Weight gain: Average gain is modest but metabolic labs should still be obtained.
Nasal congestion: Common due to α1 blockade; supportive care usually sufficient.

Drug Interactions

Strong CYP2D6 inhibitors or poor metabolizer status often require halving the iloperidone dose. Strong CYP3A4 inhibitors elevate exposure—dose reduction by ~50% is common, with QTc monitoring often considered.

Strong CYP3A4 inducers can markedly reduce serum levels and are generally avoided due to potential loss of efficacy.
Additive QTc prolongation with drugs such as amiodarone, sotalol, or methadone; ECG monitoring is often considered or alternatives may be preferred.
Concomitant antihypertensives, alcohol, or CNS depressants may potentiate hypotension and sedation.

Practice Notes

Orthostatic vitals are often checked at baseline, during titration, and after dose increases. Patient education often includes restarting titration if therapy is interrupted and reporting presyncope or palpitations.

Routine metabolic monitoring is continued even though average weight gain is limited.

References

FANAPT (iloperidone) prescribing information — DailyMed (2024)
Efficacy and safety of iloperidone in acute schizophrenia — Schizophrenia Research (2008)
Iloperidone IN THE Treatment OF Schizophrenia: AN Evidence Based Review OF ITS Place IN Therapy — Core Evidence (2016)
The American Psychiatric Association Practice Guideline for the Treatment of Patients With Schizophrenia — American Psychiatric Association (2020)Guidelineschizophreniaclinical
Iloperidone FOR Schizophrenia: Updated Systematic Review AND Meta Analysis — International Journal of Neuropsychopharmacology (2019)