鲁拉西酮:精神分裂症的新治疗选择。

IF 1.8 4区 医学 Q2 Medicine
R T Owen
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引用次数: 4

摘要

鲁拉西酮是一种新型苯并异噻唑类抗精神病药物,最近在美国被批准用于治疗精神分裂症。与许多其他第二代抗精神病药物一样,鲁拉西酮对多巴胺D(2)和5-羟色胺5-HT(2A)受体以及5-HT(7)受体具有高亲和力。它对α(1)-肾上腺素受体、组胺H(1)受体或毒蕈碱乙酰胆碱M(1)受体的亲和力可忽略不计。它在短期试验中证明了与安慰剂相比的有效性,其中两个试验包括一个活性比较物(奥氮平,喹硫平)试验组。也进行了一项短期的鲁拉西酮与齐拉西酮对慢性稳定型精神分裂症的试验。一项为期12个月的长期利培酮对照研究和开放标签研究主要调查了鲁拉西酮的安全性和耐受性。有限的证据表明,促进认知和抗抑郁的作用,尽管这些需要进一步证实。鲁拉西酮组锥体外系症状(不包括静坐症/躁动)的发生率(14.7%)高于安慰剂组(5.1%)。静坐和嗜睡是与剂量相关的不良事件。迄今为止,鲁拉西酮对体重、血糖或血脂的影响相对较小。未见QTc延长,体位性低血压不常见。在短期研究中,催乳素水平升高是剂量依赖性的,在女性中更高,总体上分别在3.7%和0.7%的鲁拉西酮和安慰剂接受者中发生。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Lurasidone: a new treatment option for schizophrenia.

Lurasidone is a novel benzoisothiazol antipsychotic that has recently been approved for the treatment of schizophrenia in the U.S. Like many other second-generation antipsychotics, it has a high affinity for dopamine D(2) and serotonin 5-HT(2A) receptors as well as a high affinity for 5-HT(7) receptors. It has negligible affinity for α(1)-adrenoceptors, histamine H(1) receptors or muscarinic acetylcholine M(1) receptors. It has demonstrated efficacy in short-term trials versus placebo, two of which included an active comparator (olanzapine, quetiapine) assay arm. A short-term, head-to-head trial of lurasidone versus ziprasidone in chronic stable schizophrenia was also conducted. A long-term, 12-month risperidone-controlled study and open-label studies primarily investigated the safety and tolerability of lurasidone. Limited evidence of procognitive and antidepressant effects was seen although these need further corroboration. The incidence of extrapyramidal symptoms (excluding akathisia/restlessness) was greater with lurasidone (14.7%) than placebo (5.1%). Akathisia and somnolence were dose-related adverse events. Lurasidone appears to have relatively little effect on weight, plasma glucose or lipids to date. No evidence of QTc prolongation was seen and orthostatic hypotension was uncommon. Raised prolactin levels in short-term studies were dose-dependent, greater in females and occurred overall in 3.7 and 0.7% of lurasidone and placebo recipients, respectively.

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来源期刊
Drugs of today
Drugs of today 医学-药学
CiteScore
3.90
自引率
0.00%
发文量
48
审稿时长
6-12 weeks
期刊介绍: An international, peer-reviewed journal publishing monographs on new products entering the market and review articles. Since its inception in 1965, Drugs of Today has established a reputation for excellence in providing physicians and other key healthcare professionals with practical, up-to-date monographs on recently approved and launched drugs.
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