Clinical Overview
Cariprazine is an atypical antipsychotic indicated for schizophrenia, manic or mixed episodes of bipolar I disorder, and depressive episodes associated with bipolar I disorder. It has a unique receptor profile as a dopamine D3/D2 receptor partial agonist with preferential binding to D3 receptors, potentially offering advantages for negative symptoms and cognitive function.
Primary Clinical Applications
Cariprazine is indicated for schizophrenia in adults, acute treatment of manic or mixed episodes of bipolar I disorder, and depressive episodes associated with bipolar I disorder. Its unique D3 receptor activity may provide particular benefits for negative symptoms of schizophrenia and cognitive function.
Mechanism and Clinical Benefits
Cariprazine acts as a partial agonist at dopamine D2 and D3 receptors and serotonin 5-HT1A receptors, and as an antagonist at 5-HT2A receptors. Its high affinity for D3 receptors distinguishes it from other antipsychotics and may contribute to its efficacy for negative symptoms and mood episodes.
Pharmacological Considerations
Cariprazine has a very long half-life (2-4 days) with active metabolites having even longer half-lives (1-3 weeks). This requires careful consideration when starting, adjusting doses, or discontinuing treatment, as effects may persist for weeks after the last dose.
Prescribing Information
Dosing & Administration
Schizophrenia – Adults:
- Initial: 1.5 mg once daily
- Day 2: May increase to 3 mg once daily
- Range: 1.5-6 mg once daily
- Maximum: 6 mg once daily
Bipolar I Disorder – Manic/Mixed Episodes:
- Initial: 1.5 mg once daily
- Day 2: Increase to 3 mg once daily
- Range: 3-6 mg once daily
- Maximum: 6 mg once daily
Bipolar I Disorder – Depressive Episodes:
- Initial: 1.5 mg once daily
- Range: 1.5-3 mg once daily
- Maximum: 3 mg once daily
Administration:
- Take once daily with or without food
- Consistent timing each day
- Effects may persist weeks after discontinuation due to long half-life
Indications
- Treatment of schizophrenia in adults
- Acute treatment of manic or mixed episodes associated with bipolar I disorder
- Treatment of depressive episodes associated with bipolar I disorder
Contraindications
- Known hypersensitivity to cariprazine or any component
- No absolute contraindications
Warnings & Precautions
- Boxed Warning: Increased mortality in elderly patients with dementia-related psychosis
- Neuroleptic malignant syndrome: Rare but serious risk
- Tardive dyskinesia: Risk with long-term use
- Metabolic changes: Monitor glucose, lipids, and weight
- Orthostatic hypotension: Monitor blood pressure
- Long half-life: Effects persist weeks after discontinuation
Drug Interactions
- Strong CYP3A4 inhibitors: Reduce cariprazine dose by 50%
- Strong CYP3A4 inducers: May require cariprazine dose increase
- CNS depressants: Enhanced sedation
Adverse Reactions
Common (≥5%):
- Extrapyramidal symptoms, akathisia, dizziness, somnolence
- Nausea, vomiting, constipation
Metabolic:
- Weight gain, hyperglycemia, dyslipidemia
Special Populations
- Hepatic Impairment: Severe impairment: not recommended
- Renal Impairment: Severe impairment (CrCl <30 mL/min): not recommended
- Elderly: Increased mortality risk in dementia-related psychosis
- Pregnancy: Category C – use only if benefits outweigh risks
- Long half-life: Consider when switching medications or discontinuing
Medical Disclaimer: This information is for educational purposes only and is not intended as medical advice. Always consult with qualified healthcare professionals before making any treatment decisions. Individual patient circumstances may vary significantly.
