Cariprazine is an atypical antipsychotic indicated for:
The exact mechanism of action of cariprazine is not fully understood. Its therapeutic effects are believed to result from partial agonist activity at central dopamine D2 and serotonin 5-HT1A receptors, along with antagonist activity at serotonin 5-HT2A receptors. Cariprazine is metabolized into two active metabolites, desmethylcariprazine (DCAR) and didesmethylcariprazine (DDCAR), which exhibit receptor binding profiles similar to the parent compound.
General Dosing Information: Cariprazine is given orally once daily and can be taken with or without food. Because of the long half-life of cariprazine and its active metabolites, changes in dose will not be fully reflected in plasma for several weeks. Prescribers should monitor patients for adverse reactions and treatment response for several weeks after starting Cariprazine and after each dosage change.
Recommended Dosage in Schizophrenia: The starting dosage of Cariprazine is 1.5 mg once daily. The recommended dosage range is 1.5 mg to 6 mg once daily. The dosage can be increased to 3 mg on Day 2. Depending upon clinical response and tolerability, further dose adjustments can be made in 1.5 mg or 3 mg increments. The maximum recommended dosage is 6 mg daily. In short-term controlled trials, dosages above 6 mg daily do not confer increased effectiveness sufficient to outweigh dose-related adverse reactions.
Recommended Dosage in Manic or Mixed Episodes Associated with Bipolar I Disorder: The starting dosage of Cariprazine is 1.5 mg once daily and should be increased to 3 mg once daily on Day 2. The recommended dosage range is 3 mg to 6 mg once daily. Depending upon clinical response and tolerability, further dose adjustments can be made in 1.5 mg or 3 mg increments. The maximum recommended dosage is 6 mg daily. In short-term controlled trials, dosages above 6 mg daily do not confer increased effectiveness sufficient to outweigh dose-related adverse reactions.
Recommended Dosage in Depressive Episodes Associated with Bipolar I Disorder (Bipolar Depression): The starting dosage of Cariprazine is 1.5 mg once daily. Depending upon clinical response and tolerability, the dosage can be increased to 3 mg once daily on Day 15. Maximum recommended dosage is 3 mg once daily.
Recommended Dosage for Adjunctive Therapy to Antidepressants for the Treatment of Major Depressive Disorder: The starting dosage of Cariprazine is 1.5 mg once daily. Depending upon clinical response and tolerability, the dosage can be increased to 3 mg once daily on Day 15. In clinical trials, dosage titration at intervals of less than 14 days resulted in a higher incidence of adverse reactions. Maximum recommended dosage is 3 mg once daily.
Strong CYP3A4 inhibitors: Reduce the dose of cariprazine by half when used together.
CYP3A4 inducers: Concomitant use is not recommended as it may reduce the effectiveness of cariprazine.
Cariprazine is contraindicated in patients with known hypersensitivity to the drug. Reported reactions include rash, itching, urticaria, and angioedema such as swelling of the tongue, lips, face, or throat.
The most common adverse effects include:
There is an established pregnancy exposure registry that monitors outcomes in women exposed to cariprazine during pregnancy. There are no adequate studies regarding the presence of cariprazine in human breast milk, its effects on the breastfed infant, or its impact on milk production.
Cerebrovascular Adverse Reactions in Elderly with Dementia-Related Psychosis: Increased risk of stroke and transient ischemic attack; use with caution.
Neuroleptic Malignant Syndrome: Discontinue treatment immediately if suspected and monitor closely.
Tardive Dyskinesia: Consider stopping therapy if symptoms develop.
Late-Occurring Adverse Reactions: Due to the long half-life, monitor patients for several weeks after initiation and after each dose adjustment.
Metabolic Changes: Regularly monitor blood glucose, lipid profile, and body weight.
Leukopenia, Neutropenia, and Agranulocytosis: Monitor complete blood count, especially in patients with a history of low WBC; discontinue if significant decline occurs.
Orthostatic Hypotension and Syncope: Monitor blood pressure and heart rate; caution in patients with cardiovascular or cerebrovascular disease.
Seizures: Use cautiously in patients with a history of seizures or conditions that lower seizure threshold.
Cognitive and Motor Impairment: Advise caution when performing activities requiring alertness, such as operating machinery.
Pediatric Use: Safety and effectiveness in pediatric patients have not been established. Antidepressants may increase the risk of suicidal thoughts and behaviors in children and adolescents.
Geriatric Use: Limited data are available in patients aged 65 years and above. Dose selection should be cautious, usually starting at the lower end, considering reduced organ function and comorbidities.
Store below 30°C in a dry place, protected from light and moisture. Keep out of reach of children.
What is Cariprazine for?
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Can Cariprazine be taken during pregnancy?
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