Cariprazine is a piperazine derivative approved by the USFDA in 2015 as a novel atypical antipsychotic drug (APD) to treat adults with schizophrenia and bipolar manic or mixed episodes in adults. However, due to the partial agonist action on dopamine D, D receptors, and serotonin 5-HT receptors as well as the antagonist effect on 5-HT, 5-HT, and H receptors, cariprazine differs pharmacologically from other APDs, both typical and atypical. Moreover, cariprazine also has a unique pharmacokinetic profile due to the formation of two clinically significant metabolites: desmethyl-cariprazine (DCAR) and desmethyl-cariprazine (DDCAR). They are eliminated by CYP3A4 and also, to a lesser extent, by CYP2D6. Here, we also review the effectiveness, safety, as well as current clinical update of cariprazine in bipolar I disorder associated with/without mania and schizophrenia through randomized and post-hoc analysis. The potential benefits of cariprazine as a promising therapeutic alternative in addressing major clinical requirements for better therapy of such severe neuropsychiatric conditions were demonstrated in this summarized review study.
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http://dx.doi.org/10.2174/1871527321666220324121935 | DOI Listing |
Harv Rev Psychiatry
November 2024
From Clinical Medicine Department, Universidad Miguel Hernández (Dr. García-Fernández); Psychiatry Department, Hospital Universitario de San Juan, Alicante, Spain (Dr. García-Fernández); CIBERSAM-ISCIII (Biomedical Research Networking Centre for Mental Health), Spain (Drs. García-Fernández, Santos, Rodriguez-Jimenez, and Romero-Ferreiro); European University of Madrid (Dr. Romero-Ferreiro); The Research Institute Hospital 12 de Octubre-Imas12 (Drs. Peñuelas-Calvo, Rodriguez-Jimenez, and Romero-Ferreiro), Madrid, Spain; Complutense University of Madrid-UCM (Drs. Peñuelas-Calvo and Rodriguez-Jimenez); Department of Medicine and Medical Specialities, University of Alcala (Dr. Álvarez-Mon); Department of Psychiatry and Mental Health. Hospital Universitario Infanta Leonor (Dr. Álvarez-Mon); Ramón y Cajal Institute of Sanitary Research-IRYCIS (Dr. Álvarez-Mon), Madrid, Spain; Department of Biomedical and Neuromotor Sciences, University of Bologna (Dr. Scala); Faculty of Health Sciences, Universidad Francisco de Vitoria (Dr. Romero-Ferreiro); CIBERESP/ISCIII (Biomedical Research Networking Centre for Epidemiology and PublicHealth/Carlos III Health Institute), Spain (Dr. Romero-Ferreiro); Center for Social and Health Research, University of Castilla-La Mancha (Dr. Jiménez López); Department of Psychiatry, Virgen de La Luz Hospital (Drs. Jiménez López and Santos); Neurobiological Research Group, Technological Institute, University of Castilla-La Mancha (Dr. Santos), Cuenca, Spain.
Background: Cariprazine (CAR), an antipsychotic with partial agonism at the D3 receptor and higher affinity than dopamine, has shown significant procognitive effects in preclinical animal studies. This study systematically reviews CAR's effects on cognitive measures in patients with schizophrenia and bipolar disorder.
Methods: Two independent reviewers systematically searched PubMed, Web of Science, Scopus, and the Cochrane Library up to May 2024, following the Preferred Reporting Items for Systematic Reviews and Meta-Analysis guidelines.
Front Psychiatry
September 2024
School of Medicine, University of Belgrade, Belgrade, Serbia.
Major depressive disorder (MDD) is among the most prevalent psychiatric conditions and a leading cause of disability worldwide. MDD presents a diverse range of symptoms that significantly impact personal, societal, and economic dimensions. Despite the availability of numerous antidepressant treatments (ADTs) targeting different molecular mechanisms, a substantial proportion of patients experience inadequate response, presenting a considerable challenge in MDD management.
View Article and Find Full Text PDFMed Sci Monit
September 2024
II Department of Psychiatry and Psychiatric Rehabilitation, Faculty of Medicine, Medical University of Lublin, Lublin, Poland.
Expert Opin Drug Saf
September 2024
Westchester Medical Center, New York Medical College, Departments of Cardiology and Medicine, Valhalla, NY, USA.
Introduction: The rising prevalence of psychiatric disorders has resulted in a significant increase in the use of antipsychotic medications. These agents may prolong the corrected QT interval (QTc), running the risk of precipitating ventricular arrhythmias, notably Torsades de Pointes (TdP). Current recommendations vary regarding the optimal approach to safe prescribing practices and QTc surveillance for antipsychotics.
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