iloperidone

General information

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

Dosing & forms

• Forms/strengths: Tablets: 1 mg, 2 mg, 4 mg, 6 mg, 8 mg, 10 mg, 12 mg.
• Frequency: 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).
• Typical range: 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).

Mechanism (brief)

Dopamine D2/D3 and serotonin 5-HT2A antagonist with high affinity for adrenergic α1 receptors, requiring slow titration.

Metabolism & Half‑life

• Metabolism: CYP2D6, CYP3A4
• Half‑life: Single-dose mean 18 h; Steady-state mean 23 h

Therapeutic Drug Monitoring (TDM)

Recommended: No

Sources

• 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)
• Iloperidone for schizophrenia: updated systematic review and meta-analysis — International Journal of Neuropsychopharmacology (2019)