阿立哌唑:一种具有独特稳健药理学的新型非典型抗精神病药物

Marilyn A Davies, Douglas J. Sheffler, Bryan L. Roth
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引用次数: 158

摘要

阿立哌唑(Abilify®)是一种非典型抗精神病药物,最近被引入临床用于治疗精神分裂症。阿立哌唑具有独特的药理学特征,包括对几种g蛋白偶联受体(gpcr)的部分激动作用[特别是多巴胺(D2)和5-HT1A]和对其他受体(特别是5-HT2A)的拮抗作用。临床试验表明,阿立哌唑对治疗精神分裂症阳性和阴性症状均有效。在短期研究中,已证实快速起效(一周内)。初步数据表明,阿立哌唑也可有效治疗躁郁症的躁狂症状。在推荐剂量下,阿立哌唑对大多数患有精神分裂症和分裂情感性障碍的成年患者似乎是安全且耐受性良好的。关于儿童和青少年使用阿立哌唑的信息有限,试点数据表明,在这一人群中应根据体重修订给药策略。在长期研究中,阿立哌唑的使用与持续的疗效、良好的依从性和增加的复发时间有关。阿立哌唑是第一种功能选择性非典型抗精神病药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Aripiprazole: A Novel Atypical Antipsychotic Drug With a Uniquely Robust Pharmacology

Aripiprazole (Abilify®) is an atypical antipsychotic drug that has been recently introduced for clinical use in the treatment of schizophrenia. Aripiprazole has a unique pharmacologic profile that includes partial agonism at several G-protein coupled receptors (GPCRs) [especially dopamine (D2) and 5-HT1A] and antagonistic action at others (especially 5-HT2A). Clinical trials indicate that aripiprazole is effective in treating the positive and negative symptoms of schizophrenia. In short-term studies rapid onset of action (within one week) has been demonstrated. Preliminary data indicate that aripiprazole may also be effective in the treatment of manic symptoms of bipolar disorder. At recommended doses, aripiprazole appears to be safe and well tolerated in most adult patients with schizophrenia and Schizoaffective disorder. There is only limited information available on the use of aripiprazole in children and adolescents, and pilot data suggest that a revised dosing strategy, based on weight, is indicated in this population. In the long-term studies, the use of aripiprazole was associated with continued efficacy, good compliance and increased time-to-relapse.

Aripiprazole represents the first functionally selective atypical antipsychotic drug.

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