Carpiniello Bernardo, Pinna Federica
Department of Public Health, Clinical and Molecular Medicine - Psychiatry Research Unit and Psychiatric Clinic, University Hospital, Cagliari, Italy.
Drug Des Devel Ther. 2016 May 24;10:1731-42. doi: 10.2147/DDDT.S86301. eCollection 2016.
Three-monthly injections of paliperidone palmitate (PP-3M) represent a new and recently introduced long-acting antipsychotic therapeutic option. This review focuses on available data relating to the efficacy and safety of PP-3M and its position in the current therapeutic scenario.
An analysis of PubMed, Scopus, and ISI Web of Knowledge databases was conducted, and all available papers on PP-3M, including poster presentations, were selected and considered for the purpose of the present review.
to date, three full papers have been published, the first, a Phase 1 randomized, open label study investigating the pharmacokinetics, safety, and tolerability of the drug; the second, a Phase 3 double blind study vs placebo focusing on efficacy and tolerability; and the last relating to the practical use of PP-3M. The five posters identified describe data reported in the above-cited papers. Overall, the pharmacokinetic findings obtained in these studies highlight the feasibility of administering PP-3M on a 3-monthly basis, subsequent to the administration of four 1-monthly injections of PP at doses 3.5 times higher than the stabilized dose of 1-monthly injections of PP (ie, 175, 300, 450, and 525 mgs). The published studies highlight a significantly longer time to relapse compared to placebo, and significantly better results compared to placebo for all secondary end-points (Positive and Negative Syndrome Scale, Clinical Global Impression-Severity Scale, Personal and Social Performance Scale scores), in addition to reasonably good safety and tolerability profiles.
PP-3M emerges as a potential candidate for use as a first-line long-acting agent in the maintenance treatment of patients with schizophrenia. Further studies should however be conducted to confirm this expectation. In view of its efficacy, tolerability, and safety, together with the longer timespan between injections, PP-3M currently represents one of the best available options, and may contribute towards addressing the issue of poor adherence, even in early psychosis.
每三个月注射一次棕榈酸帕利哌酮（PP - 3M）是一种新的且最近引入的长效抗精神病治疗选择。本综述聚焦于与PP - 3M的疗效、安全性及其在当前治疗方案中的地位相关的现有数据。
对PubMed、Scopus和ISI Web of Knowledge数据库进行了分析，为本综述选取并考虑了所有关于PP - 3M的可用论文，包括海报展示。
迄今为止，已发表了三篇完整论文，第一篇是一项1期随机、开放标签研究，调查该药物的药代动力学、安全性和耐受性；第二篇是一项3期双盲研究，与安慰剂对照，重点关注疗效和耐受性；最后一篇涉及PP - 3M的实际应用。所确定的五篇海报描述了上述论文中报告的数据。总体而言，这些研究中获得的药代动力学结果突出了在以比每月注射一次PP的稳定剂量高3.5倍的剂量（即175、300、450和525毫克）注射四次每月一次的PP后，每三个月给药一次PP - 3M的可行性。已发表的研究突出显示，与安慰剂相比，复发时间显著更长，并且在所有次要终点（阳性和阴性症状量表、临床总体印象 - 严重程度量表、个人和社会表现量表评分）方面与安慰剂相比结果显著更好，此外安全性和耐受性概况也相当良好。
PP - 3M成为精神分裂症患者维持治疗中用作一线长效药物的潜在候选药物。然而，应进行进一步研究以证实这一期望。鉴于其疗效、耐受性和安全性，以及注射间隔时间更长，PP - 3M目前是最佳可用选择之一，并且可能有助于解决依从性差的问题，即使在早期精神病阶段也是如此。
