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At a glance

Iloperidone is an atypical antipsychotic used for the treatment of schizophrenia in adults and acute treatment of manic or mixed episodes associated with bipolar I disorder in adults.

Indications
  • Treatment of schizophrenia in adults
  • Acute treatment of manic or mixed episodes associated with bipolar I disorder in adults
Pharmacology

Iloperidone shows high affinity and maximal receptor occupancy for dopamine D2 receptors in the caudate nucleus and putamen of schizophrenic patients. Improvement in cognition is attributed to high affinity for α adrenergic receptors. Iloperidone also binds with high affinity to serotonin 5-HT2a and dopamine D3 receptors, moderate affinity to D4, 5-HT6, 5-HT7 and NEα1 receptors, and weak affinity to 5-HT1A, D1 and H1 receptors.

Dosage

Adult Dose (Oral):

  • Schizophrenia: Starting: 1 mg twice daily; Recommended: 6-12 mg twice daily
  • Bipolar Mania: Starting: 1 mg twice daily; Recommended: 12 mg twice daily
  • Titrate slowly to avoid orthostatic hypotension; symptom control may be delayed during first 1-2 weeks
  • Day 1: 1 mg BID; Day 2: 2 mg BID; then increase by 2 mg/day to effective dose (max 24 mg/day)

Hepatic Impairment: Mild: No dosage adjustment; Moderate: Caution; Severe: Not recommended

Renal Dose: No dose adjustment needed (<1% excreted unchanged in urine)

Child Dose: Safety and efficacy not established

Side effects

Most Common (≥5% and 2-fold greater than placebo):

  • Dizziness
  • Dry mouth
  • Fatigue
  • Nasal congestion
  • Orthostatic hypotension
  • Somnolence
  • Tachycardia
  • Weight increased
  • Hepatic enzymes increased (in bipolar mania)
  • Hypotension (in bipolar mania)

Serious: QT prolongation, Neuroleptic Malignant Syndrome (NMS), Tardive dyskinesia, Hyperglycemia/diabetes, Dyslipidemia, Leukopenia/Neutropenia, Priapism

Use in pregnancy

Use in Pregnancy: May be unsafe; third trimester exposure may cause extrapyramidal and/or withdrawal symptoms in neonates; animal studies have shown harmful effects; doctor will weigh benefits and risks.

Precautions & warnings

Precautions:

  • Iloperidone may affect your ability to drive (dizziness, drowsiness)
  • Rise slowly to avoid orthostatic hypotension
  • May prolong QT interval; avoid with other QTc-prolonging drugs
  • May increase weight, blood sugar, cholesterol and triglycerides; eat healthy and exercise regularly
  • Neuroleptic Malignant Syndrome (NMS): Discontinue immediately
  • Tardive dyskinesia: Discontinue if clinically appropriate
  • Monitor CBC in patients with pre-existing leukopenia/neutropenia
  • Increased risk of cerebrovascular adverse reactions in elderly patients with dementia-related psychosis
Overdose effects

Overdose: May cause QT prolongation, sedation, orthostatic hypotension; provide symptomatic supportive treatment; ECG monitoring may be required.

Storage conditions

Store at controlled room temperature, 25°C; excursions permitted to 15° to 30°C.

Iloperidone — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.