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氨磺必利:进展与结果。

Amisulpride: progress and outcomes.

作者信息

Lecrubier Y

机构信息

The French Institute of Health and Medical Research, Hĵpital La Salpêtrière, Paris.

出版信息

Curr Med Res Opin. 2002;18 Suppl 3:s18-22. doi: 10.1185/030079902125001083.

Abstract

Amisulpride is a unique atypical antipsychotic that selectively blocks D2 and D3 receptors presynaptically in the frontal cortex, possibly enhancing dopaminergic transmission, and postsynaptically in the limbic areas, possibly reducing it. Thus dopaminergic over-activity in the frontal cortex, and under-activity in the limbic areas, can be treated simultaneously, alleviating both positive and negative symptoms of schizophrenia, respectively. In acute schizophrenia, amisulpride is at least as effective as haloperidol, with a greater number of patients responding to treatment as determined by Clinical Global Impression (CGI scores (p = 0.014). In addition, amisulpride is associated with a lower incidence of extrapyramidal symptoms (EPS) as determined by Simpson-Angus scores (SAS) when compared with haloperidol (p = 0.0053). Amisulpride showed similar efficacy to risperidone as determined by the Brief Psychiatric Rating Scale (BPRS) and the Positive and Negative Symptom Score (PANSS) positive subscale; a trend towards greater improvement of negative symptoms as determined by PANSS negative subscale compared with risperidone; and similar levels of EPS. Amisulpride uniquely benefits patients with negative symptoms and is the only antipsychotic to demonstrate efficacy in patients with predominantly negative symptoms. Amisulpride maintains its efficacy when used for medium/long-term treatment as demonstrated in studies of up to 12 months. Amisulpride demonstrates greater improvement in controlling symptoms compared to haloperidol. In terms of the relevance of the effects, a superiority is observed for quality of life, social adaptation and functioning as measured by the Quality of Life Scale (QLS), Clinical Glocal Impression scale (CGI) and Functional Status Questionnaire (FSQ) scales. Amisulpride also has one of the lowest potentials of all the antipsychotic agents for weight gain. The clinical evidence for amisulpride supports its earlier pre-clinical potential, showing it to be an atypical antipsychotic agent with specific clinical advantages.

摘要

氨磺必利是一种独特的非典型抗精神病药物,它能选择性地在额叶皮质突触前阻断D2和D3受体,可能增强多巴胺能传递;在边缘系统突触后阻断这些受体,可能减少多巴胺能传递。因此,额叶皮质多巴胺能活性过高和边缘系统多巴胺能活性过低的情况可同时得到治疗,分别缓解精神分裂症的阳性和阴性症状。在急性精神分裂症中,氨磺必利至少与氟哌啶醇一样有效,根据临床总体印象量表(CGI评分,p = 0.014),有更多患者对治疗有反应。此外,与氟哌啶醇相比,根据辛普森-安格斯量表(SAS)测定,氨磺必利的锥体外系症状(EPS)发生率更低(p = 0.0053)。根据简明精神病评定量表(BPRS)和阳性与阴性症状量表(PANSS)阳性分量表测定,氨磺必利显示出与利培酮相似的疗效;根据PANSS阴性分量表测定,与利培酮相比,氨磺必利有使阴性症状改善更明显的趋势;且EPS水平相似。氨磺必利对有阴性症状的患者有独特的益处,是唯一一种在以阴性症状为主的患者中显示出疗效的抗精神病药物。如长达12个月的研究所表明的,氨磺必利用于中长期治疗时能维持其疗效。与氟哌啶醇相比,氨磺必利在控制症状方面有更明显的改善。就这些效应的相关性而言,在生活质量、社会适应和功能方面观察到优越性,这些方面通过生活质量量表(QLS)、临床总体印象量表(CGI)和功能状态问卷(FSQ)量表进行测量。氨磺必利也是所有抗精神病药物中体重增加潜力最低的药物之一。氨磺必利的临床证据支持其早期临床前的潜力,表明它是一种具有特定临床优势的非典型抗精神病药物。

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