Brexpiprazole: so far so good
Brexpiprazole: so far so good
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DOI：
10.1177/2045125315614739
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发表时间：
2016-02-01
影响因子：
4.2
通讯作者：
Saha, Indranil
中科院分区：
文献类型：
--
作者：
Das, Saibal;Barnwal, Preeti;Saha, Indranil
本文介绍了一种新批准的抗精神病药布雷哌唑在治疗精神分裂症和抑郁症中的作用。该药物对5-HT 1A、5-HT 2A、D-2和α（1B，2C）受体具有高亲和力。对5-HT 1A和D-2受体显示部分激动作用，对5-HT 2A和α（1B，2C）肾上腺素能受体显示强效拮抗作用。它对D-3、5-HT 2B、5-HT 7和α（1A，1D）受体也具有一定的亲和力（拮抗作用），对H-1受体具有中等亲和力，对M1受体具有低亲和力。这些都导致在改善认知表现和睡眠模式方面的有利抗精神病药特征，以及对情感状态的影响和治疗精神分裂症和重度抑郁症核心症状的潜力，包括认知缺陷，不良反应风险低（锥体外系症状、代谢并发症、体重增加，静坐不能潜力），这是其他典型和第二代抗精神病药物常见的问题。在我们的综述中，我们试图从两项主要试验（VECTOR和BEACON）中解读布雷哌唑的药理学特征。我们还试图通过访问美国食品药品监督管理局数据库（2015年）中的产品特征总结，对布雷哌唑及其早期同类药物阿立哌唑和原型抗精神病药物氯丙嗪的药理学特征进行头对头比较，从而对布雷哌唑进行简要但详细的概述。已经讨论了与该药物相关的相关临床前和临床研究，重点是疗效和安全性问题。从迄今为止所做的研究，可以得出结论，布雷哌唑可以是一种有效的单药治疗精神分裂症，并作为辅助治疗其他抗抑郁药物在重度抑郁症。
This article describes the role of a newly approved antipsychotic agent brexpiprazole in the treatment of schizophrenia and major depressive disorder. This drug has high affinity for 5-HT1A, 5-HT2A, D-2 and alpha(1B,2C) receptors. It displays partial agonism at 5-HT1A and D-2 receptors and potent antagonism at 5-HT2A and alpha(1B,2C) adrenergic receptors. It also has some affinity (antagonism) for D-3, 5-HT2B, 5-HT7 and alpha(1A,1D) receptors, and moderate affinity for H-1 and low affinity for M1 receptors. These all lead to a favorable antipsychotic profile in terms of improvement of cognitive performance and sleep patterns, as well as effects on affective states and potential to treat core symptoms in schizophrenia and major depressive disorder, including cognitive deficits with a low risk of adverse effects (extrapyramidal symptoms, metabolic complications, weight gain, akathisia potential) that are commonly encountered with other typical and second-generation antipsychotic drugs. In our review, we have made an attempt to decipher the pharmacological profile of brexpiprazole from two major trials (VECTOR and BEACON). We have also tried to give a concise but detailed overview of brexpiprazole by head to head comparison of the pharmacological profile of brexpiprazole and its earlier congeners aripiprazole and prototype antipsychotic drug chlorpromazine by accessing individual summaries of product characteristics from the US Food and Drug Administration database, 2015. Relevant preclinical and clinical studies associated with this drug have been discussed with emphasis on efficacy and safety concerns. From the studies done so far, it can be concluded that brexpiprazole can be an effective monotherapy for schizophrenia and as an adjunct to other antidepressant medications in major depressive disorder.