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卡立普嗪综述:一种有前景的抗精神病药物

Mini Review on Cariprazine: A Promising Antipsychotic Agent.

作者信息

Patel Ashish, Patel Arya, Patel Darshini, Patel Krina, Bambharoliya Tushar

机构信息

Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology, CHARUSAT-Campus, Changa-388421, Anand, Gujarat, India.

North Carolina State University, North Carolina, USA.

出版信息

CNS Neurol Disord Drug Targets. 2023;22(2):226-236. doi: 10.2174/1871527321666220324121935.

Abstract

Cariprazine is a piperazine derivative approved by the USFDA in 2015 as a novel atypical antipsychotic drug (APD) to treat adults with schizophrenia and bipolar manic or mixed episodes in adults. However, due to the partial agonist action on dopamine D, D receptors, and serotonin 5-HT receptors as well as the antagonist effect on 5-HT, 5-HT, and H receptors, cariprazine differs pharmacologically from other APDs, both typical and atypical. Moreover, cariprazine also has a unique pharmacokinetic profile due to the formation of two clinically significant metabolites: desmethyl-cariprazine (DCAR) and desmethyl-cariprazine (DDCAR). They are eliminated by CYP3A4 and also, to a lesser extent, by CYP2D6. Here, we also review the effectiveness, safety, as well as current clinical update of cariprazine in bipolar I disorder associated with/without mania and schizophrenia through randomized and post-hoc analysis. The potential benefits of cariprazine as a promising therapeutic alternative in addressing major clinical requirements for better therapy of such severe neuropsychiatric conditions were demonstrated in this summarized review study.

摘要

卡立普嗪是一种哌嗪衍生物,于2015年被美国食品药品监督管理局批准为新型非典型抗精神病药物(APD),用于治疗成人精神分裂症以及成人双相情感障碍的躁狂或混合发作。然而,由于卡立普嗪对多巴胺D、D受体以及5-羟色胺5-HT受体具有部分激动作用,同时对5-HT、5-HT和H受体具有拮抗作用,其在药理学上与其他典型和非典型抗精神病药物有所不同。此外,由于形成了两种具有临床意义的代谢物:去甲基卡立普嗪(DCAR)和去甲基卡立普嗪(DDCAR),卡立普嗪还具有独特的药代动力学特征。它们通过CYP3A4消除,同时在较小程度上也通过CYP2D6消除。在此,我们还通过随机和事后分析回顾了卡立普嗪在伴有或不伴有躁狂的双相I型障碍以及精神分裂症中的有效性、安全性以及当前临床进展。在这项综述研究中证明了卡立普嗪作为一种有前景的治疗选择在满足此类严重神经精神疾病更好治疗的主要临床需求方面的潜在益处。

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