Central Facility of Instrumentation, School of Pharmaceutical Sciences, IFTM University, Moradabad-244001, India.
Curr Drug Discov Technol. 2020;17(1):23-29. doi: 10.2174/1570163815666181008151718.
Aripiprazole, a synthetic compound, obtained by chemical modification of the structure of quinolinone is considered as an atypical antipsychotic drug. The present review is an attempt to summarize the updated information related to reported chemistry and pharmacology of Aripiprazole.
Aripiprazole, under development by Otsuka Pharmaceutical, was approved by the U.S. Food and Drug Administration (USFDA) by the end of 2002 with an aim to treat patients with schizophrenia. This drug got approved by European Commission in February 2013 to treat the patients having severe manic episodes in bipolar I disorder Additionally, it got approval in Japan in January 2006 and in Canada in 2014. Pharmacology: Aripiprazole shows high specificity for dopamine receptor especially D2 and D3, serotonin 5-HT1A and serotonin 5-HT2A receptors, reasonable specificity for dopamine D4, serotonin 5- HT2C and 5-HT7, alpha1-adrenergic and histamine H1 receptors. It also shows moderate specificity for the serotonin reuptake. The major side effects include headache, agitation, akithesia, anxiety, tachycardia, insomnia, postural hypotension, constipation, vomiting, dizziness, nervousness and somnolence.
The present article embarks the available information on Aripiprazole with emphasis on its clinical pharmacology, mechanism of action, pharmacokinetics, pharmacodynamics, metabolism and clinical trials.
阿立哌唑是一种通过喹啉酮结构化学修饰得到的合成化合物，被认为是一种非典型抗精神病药物。本综述旨在总结有关阿立哌唑的化学和药理学的最新信息。
由大冢制药开发的阿立哌唑于 2002 年底获得美国食品和药物管理局（USFDA）批准，旨在治疗精神分裂症患者。该药物于 2013 年 2 月获得欧洲委员会批准，用于治疗双相 I 障碍中严重躁狂发作的患者。此外，它于 2006 年 1 月在日本获得批准，于 2014 年在加拿大获得批准。药理学：阿立哌唑对多巴胺受体（尤其是 D2 和 D3）、5-羟色胺 5-HT1A 和 5-HT2A 受体具有高度特异性，对多巴胺 D4、5-羟色胺 5-HT2C 和 5-HT7、α1-肾上腺素能受体和组胺 H1 受体具有合理的特异性。它还对 5-羟色胺再摄取具有中等特异性。主要副作用包括头痛、激越、静坐不能、焦虑、心动过速、失眠、体位性低血压、便秘、呕吐、头晕、紧张和嗜睡。
本文介绍了阿立哌唑的现有信息，重点介绍了其临床药理学、作用机制、药代动力学、药效学、代谢和临床试验。
