Generic
Iloperidone
2 brands available in the market
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.
Description
Iloperidone is an atypical antipsychotic that works by modulating the action of certain chemical messengers in the brain. It shows high affinity and maximal receptor occupancy for dopamine D2 receptors, serotonin 5-HT2a receptors, and α adrenergic receptors. It is effective in treating schizophrenia and bipolar mania.
Indications
- Treatment of schizophrenia in adults
- Acute treatment of manic or mixed episodes associated with bipolar I disorder in adults
Therapeutic class
Piperidinyl-benzisoxazole derivative
Pharmacological class
Atypical Antipsychotic
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.
Mechanism of action
Acts by blocking multiple receptors including dopamine D2, serotonin 5-HT2a and α adrenergic receptors, resulting in improvement of schizophrenia and mania symptoms.
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
Administration
Administer orally twice daily at approximately the same time each day; may be taken with or without food; titrate dosage slowly to avoid orthostatic hypotension.
Missed dose
If you miss a dose, take it as soon as possible; if it is almost time for your next dose, skip the missed dose; do not double the dose.
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
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
Contraindications
Contraindications:
- Known hypersensitivity to Iloperidone or any components in the formulation
Drug interactions
There are no known drug interactions and none well documented.
Food interactions
Food Interactions: Caution is advised when consuming alcohol with Iloperidone; consult your doctor.
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.
Use in lactation
Use in Lactation: No information regarding presence of iloperidone or its metabolites in human milk, effects on breastfed child, or effects on milk production; present in rat milk.
Pediatric use
Safety and effectiveness in children and adolescents have not been established.
Geriatric use
Increased incidence of cerebrovascular adverse reactions (stroke, TIA) in elderly patients with dementia-related psychosis.
Renal / hepatic impairment
Renal Impairment: No dose adjustment likely needed (<1% excreted unchanged in urine); probably safe.
Hepatic Impairment: Mild: No dosage adjustment; Moderate: Caution; Severe: Use not recommended.
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.
Chemical structure
Iloperidone