Department of Biomedical Sciences (Pharmacology Area), Faculty of Medicine and Health Sciences, University of Alcalá, Madrid, Spain.
Expert Rev Neurother. 2014 Jun;14(6):593-605. doi: 10.1586/14737175.2014.915741. Epub 2014 Apr 30.
The majority of patients with bipolar disorder spend a lot of time in depressive episodes that impose a great burden on patients, caregivers, and society and accounts for the largest part of the morbidity-mortality of the illness. Lurasidone is an atypical antipsychotic with a potent binding affinity as antagonist for D2, 5-HT2A, 5-HT7, and partial agonist at 5-HT1A receptors. Affinity for other receptors as H1 and muscarinic were negligible. Lurasidone was approved in 2010 for the treatment of schizophrenia and recently, 2013, for bipolar depression in monotherapy and an adjunct to lithium or valproate. Clinical trials have established that lurasidone adjuvant to lithium or valproate has more efficacy than the placebo and is associated with minimal weight gain and no clinically meaningful alterations in glucose, lipids, or the QT interval. Additional studies are desirable to know the clinical profile of lurasidone in long-term treatment, in patients with bipolar II disorders, and versus other antipsychotic agents.
大多数双相情感障碍患者会经历大量的抑郁发作，这给患者、护理人员和社会带来了巨大的负担，也是导致该病发病率和死亡率的主要原因。鲁拉西酮是一种非典型抗精神病药物，对 D2、5-HT2A、5-HT7 受体具有很强的拮抗亲和力，对 5-HT1A 受体具有部分激动作用。对其他受体（如 H1 和毒蕈碱）的亲和力可以忽略不计。鲁拉西酮于 2010 年获批用于治疗精神分裂症，最近于 2013 年获批用于单相双相抑郁的单药治疗以及锂盐或丙戊酸盐的辅助治疗。临床试验已经证实，鲁拉西酮作为锂盐或丙戊酸盐的辅助治疗比安慰剂更有效，且不会导致体重增加，也不会对血糖、血脂或 QT 间期产生临床上有意义的改变。需要进一步的研究来了解鲁拉西酮在长期治疗中的临床特征，包括在双相 II 型障碍患者中的应用，以及与其他抗精神病药物的比较。
