卡利拉嗪在双相情感障碍抑郁和躁狂中的应用：现状。
Cariprazine in Bipolar Depression and Mania: State of the Art.
机构信息
Institute of Psychiatry and Psychology, Department of Geriatrics, Neuroscience and Orthopedics, Fondazione Policlinico Universitario A. Gemelli IRCSS, Universita Cattolica del Sacro Cuore, Rome, Italy.
Department of Science, University of Rome "Roma Tre", Rome, Italy.
出版信息
CNS Neurol Disord Drug Targets. 2018;17(10):723-727. doi: 10.2174/1871527317666180828120256.
BACKGROUND & OBJECTIVE: Cariprazine is a piprazine derivative approved by the FDA in 2015 for the treatment of schizophrenia and bipolar manic or mixed episodes in adults. High affinity for D3 dopamine receptors and observed actions on 5HT1A, 5HT2A and alpha 1B receptors differentiate it pharmacologically from other antipsychotics. This review is a comprehensive and thorough summary of the most important findings on cariprazine use in bipolar mania and depression. Pharmacokinetics, pharmacogenetics, tolerability and safety adverse effects are discussed in this paper.
RESULTS & CONCLUSION: Moreover, the results from pivotal clinical trials are presented. Cariprazine represents an additional option for clinicians to treat patients with bipolar disorder. It shows a unique pharmacological profile and has demonstrated in randomized clinical trials efficacy and general tolerability compared to placebo in bipolar mania and seem to be a promising therapeutic option for bipolar depression.
背景与目的
卡利培嗪是一种哌嗪衍生物，于 2015 年被美国食品药品监督管理局（FDA）批准用于治疗成人精神分裂症和双相情感障碍躁狂或混合发作。其对多巴胺 D3 受体具有高亲和力，对 5HT1A、5HT2A 和 alpha 1B 受体的观察作用使其在药理学上区别于其他抗精神病药物。这篇综述全面而深入地总结了卡利培嗪在双相情感障碍躁狂和抑郁中的应用的最重要发现。本文讨论了药代动力学、药物遗传学、耐受性和安全性不良反应。
结果与结论
此外，还介绍了关键性临床试验的结果。卡利培嗪为临床医生治疗双相情感障碍患者提供了另一种选择。它具有独特的药理学特征，在随机临床试验中与安慰剂相比，在双相躁狂症中显示出疗效和总体耐受性，并且似乎是治疗双相抑郁症的一种有前途的治疗选择。
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