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精神分裂症药物的演变:聚焦多巴胺能系统。

Evolution of schizophrenia drugs: a focus on dopaminergic systems.

作者信息

Nikam Sham S, Awasthi Alok K

机构信息

Nycomed Pharma Pvt Ltd, Plot 29/30/31, Andheri East, Mumbai, India.

出版信息

Curr Opin Investig Drugs. 2008 Jan;9(1):37-46.

PMID:18183530
Abstract

Many of the drugs currently marketed for the treatment of schizophrenia are dopamine D2 receptor antagonists or partial agonists with or without mixed receptor pharmacology, and primarily treat the positive symptoms of schizophrenia. These drugs, depending on their pharmacological profile, have been categorized as typical (with low or no serotonergic component) and atypical (with a high serotonergic, 5-HT2A and 5-HT1A component) antipsychotics. Atypical antipsychotics have increased tolerability compared with typical antipsychotics, particularly against extrapyramidal side effects which are caused by D2 receptor antagonism, and an increased efficacy for the treatment of the negative symptoms associated with schizophrenia. However, over the course of treatment, adverse effects such as weight gain, metabolic disorders, QT prolongation and sexual dysfunction have been observed, and thus current research efforts are being directed to the identification of new antipsychotics that have better tolerability and efficacy against the positive and negative symptoms of schizophrenia.

摘要

目前市面上许多用于治疗精神分裂症的药物都是多巴胺D2受体拮抗剂或部分激动剂,具有或不具有混合受体药理学特性,主要用于治疗精神分裂症的阳性症状。根据其药理学特征,这些药物被分为典型抗精神病药物(血清素能成分低或无)和非典型抗精神病药物(血清素能、5-HT2A和5-HT1A成分高)。与典型抗精神病药物相比,非典型抗精神病药物具有更高的耐受性,尤其是对由D2受体拮抗作用引起的锥体外系副作用,并且在治疗与精神分裂症相关的阴性症状方面疗效增强。然而,在治疗过程中,观察到了体重增加、代谢紊乱、QT间期延长和性功能障碍等不良反应,因此目前的研究工作致力于寻找对精神分裂症的阳性和阴性症状具有更好耐受性和疗效的新型抗精神病药物。

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