Abstract
Cariprazine is currently approved for the treatment of patients with schizophrenia (USA and EU), and for manic, depressive, and episodes with mixed features in bipolar I disorder (USA): several randomized controlled studies have also explored its efficacy in patients with major depressive disorder. This review summarizes its current therapeutic uses and potential advantages for treating the main symptoms of schizophrenia, bipolar I and major depressive disorder, considering its pharmacodynamic properties, efficacy, and tolerability. Its predominantly D3 receptor preferring affinity, with functional selectivity according to the prevailing neuronal environment, contributes to its efficacy across a wide array of psychopathological symptoms (including reality distortion, disorganized thought, negative symptoms, mood disturbance, anhedonia, and cognitive impairment), and to a favorable side effect profile. Cariprazine may be a “drug of choice” in patients with predominant negative and cognitive symptoms of schizophrenia, as well as those with metabolic syndrome. Further investigation of its relative efficacy when compared to aripiprazole or other active comparators is warranted. Its effectiveness in the treatment of bipolar mania, bipolar I depression and bipolar I episodes with mixed features, with minimal accompanying metabolic changes is well-established. The longer half-life and delayed time to relapse in patients diagnosed with schizophrenia when compared to other second-generation antipsychotics represent other advantages, given the high rates of non-adherence and frequent relapses seen in clinical practice. Its efficacy in overlapping symptom domains in other major psychiatric disorders appears promising.
Highlights
Schizophrenia, bipolar disorder, and major depression are common major mental disorders which make a substantial contribution toward total disability adjusted life years
Dopamine D3 receptors have a high affinity for DA and are localized predominantly in the ventral striatum and other parts of the limbic system, whereas their distribution is low in the dorsal striatum and cortical region [15]
According to the recommendation from an International Panel reported by Fagiolini et al [43] when switching from other antipsychotic drugs to cariprazine, a cross-titration is recommended with the need to reach an effective dose (“plateau” in plasma concentration) of cariprazine before tapering or stopping the first medication; adding benzodiazepines for a short period may help in reducing rebound of symptoms; the length of the titration depends on the type of other antipsychotic, which in the case of aripiprazole is one week or less, 2–3 weeks if the main antipsychotic was risperidone or haloperidol, and longer (3–4 weeks) in the cases of olanzapine and quetiapine
Summary
Schizophrenia, bipolar disorder, and major depression are common major mental disorders which make a substantial contribution toward total disability adjusted life years Despite nosological specificity, these disorders can share mood disturbance (depression, euphoria, irritability, anhedonia, etc.), reality distortion (hallucinations, delusions), and cognitive impairment may be present even during periods of remission, exerting negative effects on social functioning, basic life skills and quality of life [1,2,3]. These disorders can share mood disturbance (depression, euphoria, irritability, anhedonia, etc.), reality distortion (hallucinations, delusions), and cognitive impairment may be present even during periods of remission, exerting negative effects on social functioning, basic life skills and quality of life [1,2,3] This overlap differs according to the severity of individual symptoms and may be due to varying degrees of genetic contributions, as indicated by twin, family, and molecular genetic studies [4,5,6,7,8]. Randomized controlled trials (RCTs) are currently exploring its efficacy as add-on therapy in patients with major depressive disorder [18]
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