Batinic Borjanka, Ristic Ivan, Zugic Milica, Baldwin David S
Clinic of Psychiatry, University Clinical Centre of Serbia, Belgrade, Serbia.
Department of Psychology, Faculty of Philosophy, University of Belgrade, Belgrade, Serbia.
Front Psychiatry. 2021 Nov 23;12:784370. doi: 10.3389/fpsyt.2021.784370. eCollection 2021.
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.
卡立普嗪目前已被批准用于治疗精神分裂症患者(美国和欧盟),以及用于治疗I型双相情感障碍的躁狂、抑郁和混合发作(美国):多项随机对照研究也探讨了其在重度抑郁症患者中的疗效。本综述总结了其目前的治疗用途以及在治疗精神分裂症、I型双相情感障碍和重度抑郁症主要症状方面的潜在优势,同时考虑了其药效学特性、疗效和耐受性。其对D3受体具有优先亲和力,并根据主要的神经元环境具有功能选择性,这有助于其在广泛的精神病理症状(包括现实扭曲、思维紊乱、阴性症状、情绪障碍、快感缺失和认知障碍)中发挥疗效,并具有良好的副作用谱。卡立普嗪可能是精神分裂症主要表现为阴性和认知症状的患者以及患有代谢综合征患者的“首选药物”。与阿立哌唑或其他活性对照药物相比,对其相对疗效进行进一步研究是有必要的。其在治疗双相躁狂、I型双相抑郁和具有混合特征的I型双相发作方面的有效性已得到充分证实,且伴随的代谢变化最小。与其他第二代抗精神病药物相比,卡立普嗪在精神分裂症患者中的半衰期更长且复发时间延迟,鉴于临床实践中观察到的高不依从率和频繁复发率,这代表了其他优势。其在其他主要精神障碍重叠症状领域的疗效似乎很有前景。