Frankel Joshua S, Schwartz Thomas L
Department of Psychiatry, SUNY Upstate Medical University, Syracuse, NY, USA.
Department of Psychiatry, SUNY Upstate Medical University, 750 E. Adams Street, Syracuse, NY 13210, USA.
Ther Adv Psychopharmacol. 2017 Jan;7(1):29-41. doi: 10.1177/2045125316672136. Epub 2016 Oct 17.
Brexpiprazole and cariprazine are the latest US Food and Drug Administration approved atypical antipsychotics available in the United States. Both function as partial agonists of the dopamine-2 receptor (DR), a mechanism of action shared with aripiprazole. However, all three differ in their affinities for the DR as well as for serotonin receptors (5-HTRs). This paper seeks to delineate these pharmacodynamic and clinical differences amongst the three dopamine partial agonist atypical antipsychotic drugs.
PubMed and clinicaltrials.gov searches were used to generate preclinical and clinical evidence for review. Data derived from animal models and human subjects were used to provide insight on clinical mechanisms and adverse effect potentials. Clinical trial data were reviewed to compare clinical efficacy and adverse effects.
Efficacies among the three drugs are comparable for their shared indications. Side-effect profile and underlying pharmacodynamic mechanism of action for each drug may differ.
Partial agonism of the DR is a similarity of the three drugs reviewed. Each drug varies in affinity for both the DR and a diverse group of 5-HTRs, generating a distinct profile of clinical indications and adverse effects for each.
布雷哌唑和卡立哌嗪是美国食品药品监督管理局最新批准的在美国可用的非典型抗精神病药物。两者均作为多巴胺2受体(DR)的部分激动剂发挥作用,这是与阿立哌唑共有的一种作用机制。然而,这三种药物对DR以及血清素受体(5 - HTRs)的亲和力各不相同。本文旨在阐述这三种多巴胺部分激动剂非典型抗精神病药物之间的这些药效学和临床差异。
利用PubMed和clinicaltrials.gov检索来获取用于综述的临床前和临床证据。来自动物模型和人类受试者的数据用于深入了解临床机制和不良反应可能性。对临床试验数据进行 reviewed 以比较临床疗效和不良反应。
这三种药物在其共同适应症方面的疗效相当。每种药物的副作用概况和潜在药效学作用机制可能不同。
DR的部分激动作用是所综述的三种药物的一个相似之处。每种药物对DR和多种5 - HTRs的亲和力各不相同,从而为每种药物产生了独特的临床适应症和不良反应概况。