关键词: brexpiprazole pharmacotherapy schizophrenia

Mesh : Humans Thiophenes / therapeutic use adverse effects pharmacology Quinolones / therapeutic use adverse effects Schizophrenia / drug therapy Antipsychotic Agents / therapeutic use adverse effects Treatment Outcome Dopamine Agonists / therapeutic use adverse effects Receptors, Dopamine D2 / agonists drug effects

来  源:   DOI:10.12740/PP/OnlineFirst/169646

Abstract:
Brexpiprazole is a new antipsychotic drug from the group of dopamine D2/D3 receptor partial agonists. It represents a development of the second-generation antipsychotics and is an important addition to the pharmacological treatment options for schizophrenia. The purpose of this article is to present, illustrated by the case of brexpiprazole, how advances in the pharmacological properties of new antipsychotics translate into improved results in the treatment of schizophrenia, not only in terms of symptom reduction, but also in terms of functional improvement. The ratio of activation to blocking of the D2/D3 receptor is lower for brexpiprazole than for aripiprazole and cariprazine, which may translate into a lower risk of akathisia. Brexpiprazole has also stronger antihistaminic activity, which is likely to be associated with a stronger sedative effect, a lower risk of akathisia, excessive agitation and insomnia. Brexpiprazole meets the traditional requirements for an antipsychotic drug\'s efficacy, i.e., compared to placebo, it brings a greater reduction in schizophrenia symptoms in short-term studies and prevents schizophrenia relapses in long-term follow-up. The highest antipsychotic efficacy was found with the highest registered dose (4 mg/day). In addition to reducing positive symptoms, brexpiprazole treatment also leads to a reduction in negative and depressive symptoms, as well as anxiety. It has also a positive effect on patients\' social and personal functioning and quality of life. This action of the drug is in line with the expectations of patients and their families regarding effective treatment. It should not only reduce symptoms, but also enable a return to health, i.e., a state that, in addition to optimal health and a sense of psychological well-being, also makes it possible to maintain proper social relations.
摘要:
Brexpiprazole是来自多巴胺D2/D3受体部分激动剂的新型抗精神病药物。它代表了第二代抗精神病药的发展,并且是精神分裂症药物治疗选择的重要补充。本文的目的是介绍,以布立哌唑为例,新的抗精神病药物的药理特性的进步如何转化为精神分裂症治疗的改善结果,不仅在减轻症状方面,而且在功能改进方面。与阿立哌唑和卡利拉嗪相比,布雷哌唑的D2/D3受体的激活与阻断比率较低,这可能会降低静坐不能的风险。Brexpiprazole还具有更强的抗组胺活性,这可能与更强的镇静作用有关,静坐不能的风险较低,过度激动和失眠。Brexpiprazole符合抗精神病药物疗效的传统要求,即,与安慰剂相比,在短期研究中,它可以使精神分裂症症状减少,并在长期随访中防止精神分裂症复发。发现最高的抗精神病药效与最高的注册剂量(4mg/天)。除了减少阳性症状,brexiprazole治疗也导致减少阴性和抑郁症状,以及焦虑。它对患者的社会和个人功能以及生活质量也有积极的影响。药物的这种作用符合患者及其家人对有效治疗的期望。它不仅应该减轻症状,而且还可以恢复健康,即,一个州,除了最佳的健康和心理幸福感,也有可能保持适当的社会关系。
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