P 90 Novel therapeutic option in the treatment of schizophrenia and bipolar disorder – cariprazine, a partial D2 and D3 receptor agonist

Abstract

Introduction Schizophrenia and bipolar disorder are generally treated by second-generation antipsychotic drugs. Although they better treat negative schizophrenic symptoms and they exert less often extrapyramidal side effects than first-generation antipschotic drugs, cardiac and metabolic adverse effects weaken their therapeutic effect. Cariprazine, a partial agonist at D2 and D3 receptors, was approved for the treatment of these diseases in September 2015. A question arises, whether this new antipsychotic drug has a sufficient therapeutic effect and few adverse effects. Material/methods Cariprazine is a second-generation antipsychotic drug with a partial agonistic effect at D2 and D3 receptors with a greater affinity for the D3 receptor. In animal experiments, it shows antipsychotic and antimanic effects. Cariprazine has two major metabolites, has a rapid absorption and has a mean half-time of 2–5 days. The most frequent adverse effects are insomnia, extrapyramidal disorders, akathisia, sedation, nausea, dizziness and constipation. Results Cariprazine has been examined in randomized, clinical studies in a phase II. The improvement of positive and negative schizophrenic symptoms was greater than that of placebo. In a clinical study, its effect in the treatment of schizophrenia was compared to that of risperidone. The therapeutic effect of cariprazine was comparable to that of risperidone, although the improvement of positive and negative schizophrenic symptoms was greater in the risperidone group. In a clinical study with patients suffering from bipolar disorder, cariprazine improved the manic symptoms after three weeks better than placebo. Adverse effects occurred in 70% of patients, above all extrapyramidal symptoms such as akathisia and tremor. Extrapyramidal side effects occurred less often than in the risperidone group. Cariprazine shows a favorable metabolic profile, i.e. it increases blood sugar and cholesterol levels to a lesser extent than other antipsychotic drugs. It is a prolactin-sparing antipsychotic drug. Conclusion Cariprazine can be used for the treatment of schizophrenia and bipolar disorder. In clinical studies, its effect is comparable to that of risperidone for the treatment of schizophrenia. Besides, it shows antimanic effects. The most frequent adverse effect is akathisia. It has a favorable metabolic profile and does not raise prolactin levels.