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鲁马替培隆:新药还是换汤不换药?

Lumateperone: New Drug or Same Old Drug With a New Dress?

出版信息

J Psychosoc Nurs Ment Health Serv. 2020 Jun 1;58(6):9-12. doi: 10.3928/02793695-20200513-01.

Abstract

Lumateperone (Caplyta) is a drug recently approved by the U.S. Food and Drug Administration for the treatment of schizophrenia. But is it a new drug with promise, or a similar drug with new wrappings? This drug, similar to other second- and third-generation serotonin dopamine antagonists, is a potent antagonist at higher serotonin 2A receptors as well as brief binding to dopamine 1 and dopamine 2 (D2) receptors, but also has partial agonism at presynaptic D2 and indirect modulation of N-Methyl-D-aspartic acid (NMDA) and alpha-amino-3-hydroxy-5-methyl-isoxazolepropionic acid (AMPA) of the glutamine receptors. The current article reviews the putative effects of this novel mechanism of action on symptoms of schizophrenia as discussed in Phase II and III trials. A case study applies the information to a clinical situation. [Journal of Psychosocial Nursing and Mental Health Services, 58(6), 9-12.].

摘要

卢美哌隆(Caplyta)是一种最近获得美国食品和药物管理局批准用于治疗精神分裂症的药物。但它是一种有前途的新药,还是一种有新包装的类似药物?这种药物与其他第二代和第三代 5-羟色胺多巴胺拮抗剂相似,是一种强效的高 5-羟色胺 2A 受体拮抗剂,以及短暂结合多巴胺 1 和多巴胺 2(D2)受体,但也具有突触前 D2 的部分激动作用,并间接调节谷氨酰胺受体的 N-甲基-D-天冬氨酸(NMDA)和α-氨基-3-羟基-5-甲基-异恶唑丙酸(AMPA)。本文综述了在 II 期和 III 期试验中讨论的这种新型作用机制对精神分裂症症状的推测作用。一个案例研究将这些信息应用于临床情况。[心理社会护理和心理健康服务杂志,58(6),9-12。]。

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