Drug Guide
Iloperidone
Classification
Therapeutic: Antipsychotic
Pharmacological: Atypical antipsychotic
FDA Approved Indications
- Schizophrenia
Mechanism of Action
Iloperidone works by selectively antagonizing dopamine D2 and serotonin 5-HT2A receptors, helping to balance neurotransmitters related to psychotic symptoms.
Dosage and Administration
Adult: Starting dose is typically 1 mg twice daily, titrated up to 12-24 mg twice daily based on response and tolerability.
Pediatric: Not approved for pediatric use.
Geriatric: Use with caution; start at lower doses and monitor closely.
Renal Impairment: Use with caution; adjust dose as needed.
Hepatic Impairment: Use with caution; dose adjustments may be necessary.
Pharmacokinetics
Absorption: Well absorbed orally.
Distribution: Extensively bound to plasma proteins.
Metabolism: Primarily metabolized by CYP3A4 and CYP2D6.
Excretion: Excreted mainly via urine and feces.
Half Life: Approximately 18-25 hours.
Contraindications
- Hypersensitivity to iloperidone or Component
Precautions
- History of hypotension, QT prolongation, seizures, misdiagnosis of Parkinson’s disease, or severe cardiac disease.
Adverse Reactions - Common
- Dizziness (Common)
- Somnolence (Common)
- Dry mouth (Common)
- Weight gain (Common)
Adverse Reactions - Serious
- QT prolongation (Rare to uncommon)
- Orthostatic hypotension (Uncommon)
- Seizures (Rare)
- Agranulocytosis (Very rare)
Drug-Drug Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) may increase iloperidone levels. CYP3A4 inducers (e.g., carbamazepine) may decrease levels.
Drug-Food Interactions
- Avoid grapefruit juice, which inhibits CYP3A4.
Drug-Herb Interactions
N/ANursing Implications
Assessment: Monitor blood pressure, heart rate, and ECG for QT prolongation. Assess mental status and mood.
Diagnoses:
- Risk of falls due to hypotension or dizziness.
- Risk of QT prolongation leading to arrhythmias.
Implementation: Administer with food to enhance absorption. Titrate slowly and monitor vital signs.
Evaluation: Effectiveness in reducing psychotic symptoms. Monitor for adverse effects.
Patient/Family Teaching
- Take medication as prescribed, even if feeling better.
- Report side effects such as dizziness, fainting, or abnormal heartbeat.
- Avoid alcohol and other CNS depressants.
- Learn to recognize signs of cardiac arrhythmias.
Special Considerations
Black Box Warnings:
- Elderly patients with dementia-related psychosis are at increased risk of death.
- QT prolongation risk.
Genetic Factors: CYP2D6 poor metabolizers may have higher plasma levels.
Lab Test Interference: May cause false-positive results in some drug screens.
Overdose Management
Signs/Symptoms: Dizziness, hypotension, tachycardia, altered mental status.
Treatment: Supportive care; monitor cardiac status; activated charcoal if early; overcorrection of hypotension with IV fluids and vasopressors as needed.
Storage and Handling
Storage: Store at room temperature away from moisture and heat.
Stability: Stable for the shelf life specified by the manufacturer.