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A systematic review of calcium channel antagonists in bipolar disorder and some considerations for their future development.
双相情感障碍中钙通道拮抗剂的系统综述及其未来发展的一些考虑。

摘要

l-type calcium channel (LTCC) antagonists have been used in bipolar disorder for over 30 years, without becoming an established therapeutic approach. Interest in this class of drugs has been rekindled by the discovery that LTCC genes are part of the genetic aetiology of bipolar disorder and related phenotypes. We have therefore conducted a systematic review of LTCC antagonists in the treatment and prophylaxis of bipolar disorder. We identified 23 eligible studies, with six randomised, double-blind, controlled clinical trials, all of which investigated verapamil in acute mania, and finding no evidence that it is effective. Data for other LTCC antagonists (diltiazem, nimodipine, nifedipine, methyoxyverapamil and isradipine) and for other phases of the illness are limited to observational studies, and therefore no robust conclusions can be drawn. Given the increasingly strong evidence for calcium signalling dysfunction in bipolar disorder, the therapeutic candidacy of this class of drugs has become stronger, and hence we also discuss issues relevant to their future development and evaluation. In particular, we consider how genetic, molecular and pharmacological data can be used to improve the selectivity, efficacy and tolerability of LTCC antagonists. We suggest that a renewed focus on LTCCs as targets, and the development of 'brain-selective' LTCC ligands, could be one fruitful approach to innovative pharmacotherapy for bipolar disorder and related phenotypes.

译文

L 型钙通道 (LTCC) 拮抗剂已经在双相情感障碍中使用了 30 多年,但没有成为既定的治疗方法。发现 LTCC 基因是双相情感障碍的遗传病因和相关表型的一部分,这重新点燃了人们对这类药物的兴趣。因此,我们对 LTCC 拮抗剂在治疗和预防双相情感障碍方面进行了系统综述。我们确定了 23 项合格的研究,进行了 6 项随机、双盲、对照的临床试验,所有这些试验都调查了维拉帕米在急性躁狂症中的作用,但没有发现有效的证据。其他 LTCC 拮抗剂 (地尔硫卓、尼莫地平、硝苯地平、甲氧维拉帕米和伊拉地平) 和疾病其他阶段的数据仅限于观察性研究,因此无法得出可靠的结论。鉴于双相情感障碍中钙信号功能障碍的证据越来越强,这类药物的治疗候选资格变得越来越强,因此我们也讨论了与它们未来发展和评估相关的问题。特别是,我们考虑如何利用遗传、分子和药理学数据来提高 LTCC 拮抗剂的选择性、有效性和耐受性。我们认为,重新关注作为靶点的 LTCC,以及 “脑选择性” LTCC 配体的发展,可能是双相情感障碍和相关表型创新药物治疗的一个富有成效的方法。

Calcium Channel Antagonists

神经 阻滞剂 治疗药物
概述  :  

 钙通道拮抗剂,也叫钙通道阻滞剂,主要通过阻断心肌和血管平滑肌细胞膜上的钙离子通道,抑制细胞外钙离子内流,使细胞内钙离子水平降低而引起心血管等组织器官功能改变的药物。 作用部位和机制 ①通过细胞膜钙离子通道的钙离子流入。②抑制或减少了对钙离子敏感蛋白与钙离子的连接。这些敏感蛋白即就是心肌中原肌球蛋白,以及血管平滑肌中的钙调节物。⑧抑制或减少了钙离子在其储存部位,诸如肌浆网的钙离子触发的钙释放。④减少钙离子蛋白复合物的调节作用。 临床应用 冠心

calcium ['kælsɪəm]   ['kælsɪəm] 

       n. [化学]

       In fact, they may do your body harm, since chocolate can take away what calcium you do have. 事实上,他们可能会做你的身体伤害,因为确实巧克力可以导致钙损失

 

channel['tʃænl] 

       n. (美)沙内乐(人名)

n. 海峡;通道;航道;(电视)频道,(广播)波段;(交流)途径

v. 引导,开导;输送,传送;形成河道

       What channel do you like to watch best? 你最喜欢看哪一个频道的节目?

 

antagonist [æn'tæg(ə)nɪst]   [æn'tæɡənɪst] 

       n. 敌手;[解剖] 对抗肌;[生化] 拮抗物;反协同试剂

       He wondered what his antagonist was doing . 他不知道他的敌手在做些什么。

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