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舍吲哚用于精神分裂症的治疗。

Sertindole in the management of schizophrenia.

作者信息

Juruena Mario F, de Sena Eduardo Pondé, de Oliveira Irismar Reis

机构信息

Stress and Affective Disorders Programme, Department of Neuroscience and Behaviour, Faculty of Medicine of Ribeirao Preto, University of Sao Paulo, Sao Paulo, Brazil.

出版信息

J Cent Nerv Syst Dis. 2011 May 17;3:75-85. doi: 10.4137/JCNSD.S5729. Print 2011.

Abstract

Nowadays, new schizophrenia treatments are more ambitious than ever, aiming not only to improve psychotic symptoms, but also quality of life and social reinsertion. Our objective is to briefly but critically review the diagnosis of schizophrenia, the atypical antipsychotics sertindole's pharmacology, safety and status, and mainly evaluate the effects of sertindole compared with other second generation antipsychotics for people with schizophrenia and schizophrenia-like psychosis. In vitro studies showed that sertindole exerts a potent antagonism at serotonin 5-HT2A, 5-HT2C, dopamine D2, and αl adrenergic receptors. Sertindole offers an alternative treatment option for refractory patients given its good EPS profile, favorable metabolic profile, and comparable efficacy to risperidone. Due to cardiovascular safety concerns, sertindole is available as a second-line choice for patients intolerant to other antipsychotic agents. Further clinical studies, mainly comparisons with other second-generation antipsychotic agents, are needed to define the role of sertindole in the treatment of schizophrenia.

摘要

如今,新型精神分裂症治疗方法比以往任何时候都更具雄心,不仅旨在改善精神病症状,还致力于提高生活质量和促进社会融入。我们的目标是简要且批判性地回顾精神分裂症的诊断、非典型抗精神病药物舍吲哚的药理学、安全性及现状,主要评估舍吲哚与其他第二代抗精神病药物相比,对精神分裂症患者及精神分裂症样精神病患者的疗效。体外研究表明,舍吲哚对5-羟色胺5-HT2A、5-HT2C、多巴胺D2和α1肾上腺素能受体具有强效拮抗作用。鉴于其良好的锥体外系反应(EPS)特征、有利的代谢特征以及与利培酮相当的疗效,舍吲哚为难治性患者提供了一种替代治疗选择。由于心血管安全性问题,对于不耐受其他抗精神病药物的患者,舍吲哚作为二线选择药物。需要进一步的临床研究,主要是与其他第二代抗精神病药物进行比较,以确定舍吲哚在精神分裂症治疗中的作用。

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