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长效第二代抗精神病药:药物更新及比较

Long-Acting Injectable Second-Generation Antipsychotics: An Update and Comparison Between Agents.

机构信息

Department of Pharmacotherapy, University of North Texas System College of Pharmacy (UNTSCP), University of North Texas Health Science Center (UNTHSC), 3500 Camp Bowie Blvd., Fort Worth, TX, 76107, USA.

出版信息

CNS Drugs. 2018 Mar;32(3):241-257. doi: 10.1007/s40263-018-0508-6.

Abstract

Schizophrenia is a chronic medical condition with periods of remission and relapses over a patient's lifetime. Antipsychotic medications represent the mainstay of treatment for this disease. Long-acting injectable (LAI) formulations of antipsychotics are an attractive alternative to their oral counterparts, as they enhance patient adherence. A number of second-generation antipsychotics (SGAs) are available in LAI formulations. These include paliperidone, aripiprazole, olanzapine, and risperidone. This article reviews the most recently developed and approved of these formulations-aripiprazole monohydrate, aripiprazole lauroxil, and paliperidone palmitate. While all were initially available as once-monthly formulations, a paliperidone palmitate 3-monthly injection formulation has been approved and is the first LAI agent to extend the dosing administration beyond the typical monthly time period. In addition, aripiprazole lauroxil every 6-week and 8-week administration preparations have been developed. LAI preparations of the SGAs have all demonstrated superiority over placebo and are comparable to their oral counterparts in terms of safety and tolerability, if injection site reactions are not taken into account. First-generation antipsychotic LAI preparations (e.g., haloperidol decanoate) have recently been compared with SGA LAI agents, and both formulations demonstrated comparable efficacy with the expected adverse events seen with each drug. Despite their availability, barriers to the use of LAIs remain. Education of both patients and clinicians on the use of LAI formulations and the continued development of these agents are important steps in ensuring these medications are available to the patients they would be most likely to benefit.

摘要

精神分裂症是一种慢性疾病,患者一生中会有缓解期和复发期。抗精神病药物是治疗这种疾病的主要方法。长效注射(LAI)制剂是口服制剂的一种有吸引力的替代方法,因为它们可以提高患者的依从性。一些第二代抗精神病药物(SGAs)有 LAI 制剂。其中包括帕利哌酮、阿立哌唑、奥氮平利培酮。本文综述了这些制剂中最新开发和批准的制剂——阿立哌唑水合物、阿立哌唑月桂酸酯和棕榈酸帕利哌酮。虽然最初都是每月一次的制剂,但棕榈酸帕利哌酮每 3 个月注射一次的制剂已经获得批准,是第一种将给药间隔延长至典型每月时间周期以上的 LAI 药物。此外,还开发了每 6 周和 8 周给药的阿立哌唑月桂酸酯制剂。SGAs 的 LAI 制剂均优于安慰剂,在安全性和耐受性方面与口服制剂相当,如果不考虑注射部位反应的话。第一代抗精神病药 LAI 制剂(如氟哌啶醇癸酸酯)最近与 SGA LAI 制剂进行了比较,两种制剂均显示出与每种药物预期不良反应相当的疗效。尽管这些制剂已经上市,但使用 LAI 制剂仍然存在障碍。对患者和临床医生进行 LAI 制剂使用方面的教育,以及继续开发这些制剂,是确保这些药物能够提供给最有可能受益的患者的重要步骤。

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