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布雷哌唑:部分多巴胺激动剂领域的新进展。

Brexpiprazole: a new leaf on the partial dopamine agonist branch.

作者信息

Hope Judy, Castle David, Keks Nicholas A

机构信息

Senior Lecturer, Monash University, Eastern Health and Centre for Mental Health Education and Research at Delmont Private Hospital, Melbourne, VIC, Australia.

Professor, St. Vincent's Hospital, University of Melbourne, Melbourne, VIC, Australia.

出版信息

Australas Psychiatry. 2018 Feb;26(1):92-94. doi: 10.1177/1039856217732473. Epub 2017 Oct 10.

Abstract

OBJECTIVES

Brexpiprazole is a new dopamine partial agonist antipsychotic in the same class as aripiprazole. This paper will briefly review brexpiprazole and compare it with aripiprazole.

CONCLUSIONS

Brexpiprazole and aripiprazole are both partial agonists at dopamine D, and serotonin 5-HT and antagonists at serotonin 5-HT and noradrenergic α receptors. However, the two drugs are significantly different in potencies at various receptors; neurochemical profiles predict that brexpiprazole may be comparable with aripiprazole in its antipsychotic efficacy but may cause less akathisia, extrapyramidal side effects (EPS) and activation. In pivotal trials brexpiprazole demonstrated antipsychotic efficacy in short and long-term studies; it was also found to be an effective adjunct in patients with major depression resistant to antidepressants. Akathisia can occur early in treatment with brexpiprazole, as can minor weight gain and prolactin elevation. Indirect data extrapolations from pivotal studies suggest that brexpiprazole and aripiprazole have comparable efficacy but brexpiprazole may cause less akathisia. Like aripiprazole, brexpiprazole has been approved in the USA for use in schizophrenia and antidepressant-resistant depression. Although much more clinical experience is needed, brexpiprazole appears to be distinct from aripiprazole and a promising new 'metabolically-friendly' antipsychotic option for treatment of psychoses and mood disorders.

摘要

目的

布雷哌唑是一种新型多巴胺部分激动剂抗精神病药物,与阿立哌唑属于同一类别。本文将简要回顾布雷哌唑并将其与阿立哌唑进行比较。

结论

布雷哌唑和阿立哌唑均为多巴胺D、5-羟色胺5-HT的部分激动剂,以及5-羟色胺5-HT和去甲肾上腺素能α受体的拮抗剂。然而,这两种药物在各受体上的效价存在显著差异;神经化学特征预测,布雷哌唑在抗精神病疗效上可能与阿立哌唑相当,但可能引起较少的静坐不能、锥体外系副作用(EPS)和激活反应。在关键试验中,布雷哌唑在短期和长期研究中均显示出抗精神病疗效;还发现它对难治性抑郁症患者是一种有效的辅助药物。使用布雷哌唑治疗早期可能出现静坐不能,以及轻微体重增加和催乳素升高。关键研究的间接数据推断表明,布雷哌唑和阿立哌唑疗效相当,但布雷哌唑可能引起较少的静坐不能。与阿立哌唑一样,布雷哌唑已在美国被批准用于治疗精神分裂症和难治性抑郁症。尽管还需要更多的临床经验,但布雷哌唑似乎与阿立哌唑不同,是一种有前景的新型“代谢友好型”抗精神病药物,可用于治疗精神病和情绪障碍。

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