Second-generation (atypical) antipsychotic
Partial agonist at dopamine D2 and D3 receptors (with preferential binding to D3), and serotonin 5-HT1A receptors; antagonist at serotonin 5-HT2B and 5-HT2A receptors. D3 activity may contribute to cognitive and mood-related effects.
Schizophrenia, bipolar I disorder (acute manic or mixed episodes), adjunctive treatment of major depressive disorder (MDD)
Bipolar depression, borderline personality disorder, treatment-resistant depression
Oral capsules (1.5 mg, 3 mg, 4.5 mg, 6 mg)
1.5 mg p.o. daily; may increase to 3 mg on day 2, then titrate by 1.5–3 mg increments based on tolerability and response
1.5–6 mg/day
Long half-life (~2–4 days for cariprazine; ~1–3 weeks for active metabolite); metabolized via CYP3A4; steady state may take several weeks
Akathisia, insomnia, nausea, constipation, restlessness, extrapyramidal symptoms (EPS), anxiety
Tardive dyskinesia, impulse control problems, neuroleptic malignant syndrome (NMS), orthostatic hypotension
Monitor weight, lipids, fasting glucose, and EPS symptoms every 3–6 months
Increased risk of mortality in elderly patients with dementia-related psychosis
Cariprazine should be used cautiously in individuals with Parkinson’s disease (PD), as its dopaminergic activity may exacerbate motor symptoms. In Alzheimer’s disease (AD) and other dementias, cariprazine is not FDA-approved and carries the class warning for increased mortality; however, it may be used off-label in select cases for agitation with careful monitoring. Dose adjustments are recommended in patients with moderate hepatic impairment; it is not recommended in severe hepatic or renal impairment. Due to its long half-life and delayed steady-state, changes in dose may take several weeks to fully manifest clinically, necessitating slow titration and patient education.