School of Pharmacy, University of Missouri-Kansas City, USA.
Clin Ther. 2012 May;34(5):1023-40. doi: 10.1016/j.clinthera.2012.03.002. Epub 2012 Apr 10.
Schizophrenia and bipolar disorder are both prevalent types of psychiatric illness in the United States. As second-generation antipsychotics have become a more viable first-line treatment option, their use has been associated with a new era of adverse events (AEs), most notably metabolic and cardiovascular concerns. Although treatment options for schizophrenia and bipolar disorder have arguably improved, there continues to be a need for medications that achieve and maintain desired efficacy with minimal AEs.
This article serves as a comprehensive review of the pharmacologic profile of the second-generation antipsychotic asenapine, as well as a review of its efficacy and safety profiles based on the findings from clinical trials in schizophrenia and bipolar disorder.
Searches of Ovid MEDLINE, EMBASE, and IDIS were conducted (January 1996 to November 2011) to identify clinical studies and other primary literature sources with the following search terms: asenapine, bipolar disorder, antipsychotic, psychosis, dopamine, and schizophrenia. Only studies of asenapine and placebo and/or active-comparator arms were included.
The literature search yielded 67 unique articles, including review articles, which were excluded. The efficacy of asenapine was reported in 3 clinical studies in patients with schizophrenia, 1 each in acute and long-term settings, measured as significant changes in Positive and Negative Syndrome Scale scores over 6 and 52 weeks. Asenapine also had reported efficacy in the prevention of relapse in schizophrenia during a 26-week extension study. In addition, efficacy of asenapine was reported in 2 studies in acute mania as well as extension phases of both 9 and 40 weeks, as determined by significant changes in Young Mania Rating Scale scores. The most commonly reported AEs in these studies were somnolence (13%-24%), extrapyramidal symptoms (EPS) (7%-12%), and dizziness (11%).
The findings from multiple studies have suggested that asenapine is efficacious in the acute treatment of schizophrenia. Asenapine has reported long-term efficacy for this indication and the potential to reduce the incidence of relapse. Asenapine efficacy was also reported in the treatment of acute manic or mixed states associated with bipolar I disorder. Asenapine had an acceptable safety profile across the different disease states studied, although it was not devoid of metabolic and EPS-related AEs.
精神分裂症和双相情感障碍是美国常见的精神疾病类型。随着第二代抗精神病药物成为更可行的一线治疗选择，其应用与新的不良反应（AE）时代相关联，尤其是代谢和心血管方面的关注。尽管精神分裂症和双相情感障碍的治疗选择可能已经得到改善，但仍需要具有最小不良反应的药物来实现和维持所需的疗效。
本文全面综述第二代抗精神病药阿塞那平的药理学特征，并根据精神分裂症和双相情感障碍的临床试验结果综述其疗效和安全性特征。
在 Ovid MEDLINE、EMBASE 和 IDIS 中进行了检索（1996 年 1 月至 2011 年 11 月），以确定具有以下检索词的临床研究和其他主要文献来源：阿塞那平、双相情感障碍、抗精神病药、精神病、多巴胺和精神分裂症。仅纳入了阿塞那平和安慰剂和/或活性对照臂的研究。
文献检索得到 67 篇独特的文章，其中包括综述文章，这些文章被排除在外。在精神分裂症患者中，有 3 项临床研究报告了阿塞那平的疗效，其中 1 项在急性和长期环境中进行，以阳性和阴性综合征量表评分在 6 和 52 周时的显著变化来衡量。在一项为期 26 周的扩展研究中，阿塞那平还报告了预防精神分裂症复发的疗效。此外，在急性躁狂的 2 项研究以及 9 周和 40 周的扩展阶段中，也报告了阿塞那平的疗效，以 Young 躁狂评定量表评分的显著变化来衡量。这些研究中最常报告的不良反应为嗜睡（13%-24%）、锥体外系症状（EPS）（7%-12%）和头晕（11%）。
多项研究的结果表明，阿塞那平在精神分裂症的急性治疗中是有效的。阿塞那平对这一适应证具有长期疗效，并有降低复发率的潜力。阿塞那平在治疗与双相情感障碍 I 型相关的急性躁狂或混合状态时也具有疗效。在研究的不同疾病状态中，阿塞那平的安全性特征可接受，尽管它并非没有代谢和 EPS 相关的不良反应。
