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利培酮:综述

Risperidone: a review.

作者信息

Möller Hans-Jürgen

机构信息

Department of Psychiatry, Ludwig-Maximilians-University, Nussbaumstrasse 7, 80336 Munich, Germany.

出版信息

Expert Opin Pharmacother. 2005 May;6(5):803-18. doi: 10.1517/14656566.6.5.803.

Abstract

When the risk of agranulocytosis associated with clozapine, the prototype of the second-generation neuroleptics, became apparent, its prescription was restricted to patients refractory to classical neuroleptics such as chlorpromazine and haloperidol. This stimulated the development of several novel second-generation antipsychotics with a clinical profile similar to that of clozapine. These novel antipsychotics, which include risperidone, olanzapine and others, are characterised by different pharmacological structures, and also to a certain degree by different pharmacological mechanisms. Following the increased research on the novel second-generation antipsychotics, it became apparent that they not only have the advantage of better extrapyramidal tolerability than the classical neuroleptics, but also have a broader efficacy spectrum (i.e., advantages in the treatment of negative and depressive symptoms and cognitive disturbances in the context of schizophrenia). Risperidone was specifically designed by Paul Janssen as a combined 5-HT2A and D2 receptor antagonist, thus following the pharmacological mechanism thought to be responsible for the antipsychotic effects of clozapine. After its advent in the 1990s as the first novel second-generation antipsychotic, risperidone achieved worldwide acceptance. The following review gives an overview of the huge clinical database available for risperidone in the field of schizophrenia.

摘要

当第二代抗精神病药物的原型氯氮平所关联的粒细胞缺乏症风险变得明显时,其处方被限制用于对氯丙嗪和氟哌啶醇等经典抗精神病药物难治的患者。这刺激了几种临床特征与氯氮平相似的新型第二代抗精神病药物的研发。这些新型抗精神病药物,包括利培酮、奥氮平及其他药物,具有不同的药理结构,在一定程度上也有不同的药理机制。随着对新型第二代抗精神病药物研究的增加,很明显它们不仅具有比经典抗精神病药物更好的锥体外系耐受性优势,而且有更广泛的疗效谱(即在精神分裂症背景下治疗阴性和抑郁症状以及认知障碍方面的优势)。利培酮是由保罗·扬森专门设计的一种5-HT2A和D2受体联合拮抗剂,因此遵循了被认为是氯氮平抗精神病作用基础的药理机制。20世纪90年代作为首个新型第二代抗精神病药物问世后,利培酮在全球获得认可。以下综述概述了精神分裂症领域中可用于利培酮的庞大临床数据库。

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