Misiak Błażej, Bieńkowski Przemysław, Samochowiec Jerzy
Katedra i Zakład Genetyki, Uniwersytet Medyczny im. Piastów Śląskich we Wrocławiu.
Katedra i Klinika Psychiatrii, Warszawski Uniwersytet Medyczny.
Psychiatr Pol. 2018 Dec 29;52(6):971-981. doi: 10.12740/PP/OnlineFirst/80710.
Although the development of second-generation antipsychotics was a cornerstone in the treatment of schizophrenia, several unmet treatment needs in the field still exist. It is particularly important to note that available antipsychotics have limited efficacy in the treatment of negative symptoms and cognitive impairment. At this point, it should be noted that primary negative symptoms, i.e., those that are not due to depression, extrapyramidal symptoms or psychotic withdrawal, might affect even one-fourth of patients with schizophrenia and are associated with poor clinical and functional outcomes. Cariprazine, is an emerging antipsychotic drug, D3/D2 receptor partial agonist, with affinity to several serotonin receptors. In this article, we provide an overview of pharmacokinetic and pharmacodynamic properties of cariprazine, showing its unique receptor profile. Next, we discuss results of double-blind, placebo-controlled, randomized clinical trials and post hoc analyses of cariprazine that have been published to date. These studies have provided evidence for efficacy of cariprazine in the treatment of schizophrenia exacerbations compared to placebo, with safety and good tolerability. In addition, one clinical trial published to date revealed superior efficacy of cariprazine compared to risperidone in the treatment of predominant negative symptoms that had been also associated with concomitant improvement of functional performance. Overall, current evidence in the field supports the use of cariprazine in exacerbation of schizophrenia and suggests promising efficacy in the treatment of predominant negative symptoms.
尽管第二代抗精神病药物的研发是精神分裂症治疗的基石,但该领域仍存在一些未满足的治疗需求。尤其需要注意的是,现有的抗精神病药物在治疗阴性症状和认知障碍方面疗效有限。此时,应注意原发性阴性症状,即那些并非由抑郁、锥体外系症状或精神病性退缩引起的症状,可能影响甚至四分之一的精神分裂症患者,并与不良的临床和功能结局相关。卡立哌嗪是一种新兴的抗精神病药物,是D3/D2受体部分激动剂,对多种5-羟色胺受体具有亲和力。在本文中,我们概述了卡立哌嗪的药代动力学和药效学特性,展示了其独特的受体特征。接下来,我们讨论了迄今为止已发表的卡立哌嗪双盲、安慰剂对照、随机临床试验及事后分析的结果。这些研究提供了证据,表明与安慰剂相比,卡立哌嗪在治疗精神分裂症急性加重方面有效,且安全性良好、耐受性佳。此外,迄今为止发表的一项临床试验显示,与利培酮相比,卡立哌嗪在治疗以阴性症状为主的患者方面疗效更优,且这也与功能表现的改善相关。总体而言,该领域目前的证据支持卡立哌嗪用于精神分裂症急性加重的治疗,并表明其在治疗以阴性症状为主的患者方面具有良好的疗效前景。