Overview
Cariprazine is an atypical antipsychotic used for schizophrenia, bipolar disorder, and as adjunctive treatment for major depressive disorder. It functions as a partial agonist at dopamine D2/D3 receptors and serotonin 5-HT1A receptors with antagonist activity at other serotonin receptors. The medication requires careful titration and monitoring for metabolic, neurological, and cardiovascular effects.
Mechanism of Action
Cariprazine acts as a partial agonist at dopamine D2 and D3 receptors with high binding affinity, and at serotonin 5-HT1A receptors. It functions as an antagonist at 5-HT2B and 5-HT2A receptors with moderate to high affinity, and binds to histamine H1 receptors. This multimodal receptor profile contributes to its antipsychotic, mood-stabilizing, and antidepressant effects.
Indications
- Treatment of schizophrenia in adult and pediatric patients 13 years and older
- Acute treatment of manic or mixed episodes associated with bipolar I disorder in adult and pediatric patients 10 years and older
- Treatment of depressive episodes associated with bipolar I disorder (bipolar depression) in adult patients
- Adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD) in adult patients
Common Doses
- 1.5 mg
- 3 mg
- 4.5 mg
- 6 mg
Dosage
Initial dose typically 1.5 mg daily, titrated based on indication and tolerability. Maximum recommended dose is 6 mg daily. Requires gradual titration with dose adjustments based on clinical response and tolerability.
Contraindications
- History of hypersensitivity reaction to cariprazine (rash, pruritus, urticaria, angioedema)
Side Effects
- Extrapyramidal symptoms
- Akathisia
- Weight gain
- Sedation/somnolence
- Insomnia
- Nausea
- Constipation
- Dyspepsia
- Increased appetite
- Anxiety
- Restlessness
- Dizziness
- Orthostatic hypotension
- Metabolic changes
- Tardive dyskinesia
- Neuroleptic malignant syndrome
Interactions
- Strong or moderate CYP3A4 inhibitors: Increase cariprazine exposure - requires dosage reduction
- CYP3A4 inducers: Not recommended due to unpredictable effects on active metabolites
Counseling Points
- Take consistently with or without food
- Report any signs of infection, fever, or sore throat immediately
- Monitor for mood changes, suicidal thoughts, or unusual behaviors
- Be aware of potential sedation and avoid driving until effects known
- Report any involuntary movements, muscle stiffness, or fever
- Regular monitoring of weight, blood glucose, and lipids recommended
- Avoid sudden position changes to prevent dizziness
- Inform all healthcare providers about all medications being taken