Istituto di Ricerche Farmacologiche Mario Negri, Via La Masa 19, Milan 20156, Italy.
Expert Opin Drug Metab Toxicol. 2011 Jul;7(7):829-46. doi: 10.1517/17425255.2011.575061. Epub 2011 Apr 8.
The search for drugs that reduce psychotic symptoms, with minimal adverse effects, has led to the development of new agents that act somewhat differently from their older antipsychotic counterparts. These agents, which include aripiprazole, lurasidone and perospirone, act by targeting both D₂ and 5-HT(1A) receptors, in addition to other characteristic receptors.
This article covers the pharmacokinetics and metabolism of aripiprazole, perospirone, lurasidone and cariprazine. The review also describes the effects of physiological and pathological variables on these drugs as well as potential drug interactions. The author provides the reader with knowledge of the fundamental pharmacokinetic characteristics and metabolic pathways of these new antipsychotics, emphasizing the clinically important common features and differences compared to other older agents.
Aripiprazole, perospirone, lurasidone and cariprazine share some of the pharmacokinetic characteristics of older, lipophilic antipsychotics and, like these, each has some distinct pharmacokinetic features that are clinically beneficial and some that are not. We await the results of future practical effectiveness trials of these new antipsychotics and their follow-on derivatives to learn more about their benefit/risk profile compared with established antipsychotics. It is hoped that some of these newer antipsychotics will not only increase the range of pharmacotherapeutic options, but decisively improve the expectations of psychotherapy for schizophrenia.
寻找具有最小不良反应的可减少精神病症状的药物,导致了新型药物的开发,这些药物与较老的抗精神病药物作用方式略有不同。这些药物包括阿立哌唑、鲁拉西酮和哌罗匹隆,除了其他特征性受体外,还作用于 D₂ 和 5-HT(1A)受体。
本文涵盖了阿立哌唑、哌罗匹隆、鲁拉西酮和卡利哌嗪的药代动力学和代谢。该综述还描述了生理和病理变量对这些药物的影响以及潜在的药物相互作用。作者为读者提供了对这些新型抗精神病药物基本药代动力学特征和代谢途径的了解,强调了与其他较老药物相比,这些药物具有临床重要的共同特征和差异。
阿立哌唑、哌罗匹隆、鲁拉西酮和卡利哌嗪与较老的亲脂性抗精神病药物具有一些共同的药代动力学特征,与这些药物一样,每种药物都具有一些独特的药代动力学特征,这些特征在临床上是有益的,但也有一些是不利的。我们期待这些新型抗精神病药物及其后续衍生物的未来实际疗效试验的结果,以了解它们与已建立的抗精神病药物相比的获益/风险状况。希望其中一些新型抗精神病药物不仅能增加治疗选择范围,而且能显著改善精神分裂症的心理治疗预期。