Emsley Robin, Kilian Sanja
Department of Psychiatry, Faculty of Medicine and Health Sciences, Stellenbosch University, Cape Town, South Africa.
Neuropsychiatr Dis Treat. 2018 Jan 5;14:205-223. doi: 10.2147/NDT.S139633. eCollection 2018.
The course of schizophrenia is characterized by multiple relapses, incomplete remission of symptoms, enduring cognitive deficits, and social and occupational functional impairments. Nonadherence to antipsychotic medication is a major determinant of this poor outcome. Long-acting injectable antipsychotics were developed specifically to address the nonadherence problem and are increasingly considered as an early treatment option, in an attempt to prevent accruing morbidity. This review focuses on paliperidone palmitate, the long-acting injectable (LAI) formulation of paliperidone. After considering the pharmacology of paliperidone palmitate, we review the randomized controlled trials, as well as pertinent observational, pragmatic studies for paliperidone once-monthly injections in schizophrenia. Finally, we review the recently introduced 3-monthly formulation of paliperidone palmitate. Taken together, the studies indicate that paliperidone palmitate (PP) has good efficacy compared with placebo and comparable with other antipsychotics including risperidone. The tolerability profile of PP is similar to that of risperidone, with the most important side effects being prolactin elevation, weight gain, and extrapyramidal symptoms. Advantages of PP include the extensive research database and clinical experience with paliperidone and its parent compound risperidone, the availability of different LAI formulations (once-monthly, 3-monthly, and perhaps even longer acting formulations in future), and the novel dose initiation procedure that provides rapid onset of action without the need for oral antipsychotic supplementation.
精神分裂症的病程特点为多次复发、症状不完全缓解、持续存在认知缺陷以及社会和职业功能受损。不坚持服用抗精神病药物是导致这种不良结局的主要决定因素。长效注射用抗精神病药物专门为解决服药依从性问题而研发，并且越来越多地被视为一种早期治疗选择，旨在预防疾病的累积。本综述聚焦于棕榈酸帕利哌酮，即帕利哌酮的长效注射剂型。在考量棕榈酸帕利哌酮的药理学特性后，我们回顾了随机对照试验以及关于每月注射一次帕利哌酮治疗精神分裂症的相关观察性、实用性研究。最后，我们回顾了最近推出的每三个月注射一次的棕榈酸帕利哌酮剂型。综合来看，研究表明棕榈酸帕利哌酮（PP）与安慰剂相比疗效良好，且与包括利培酮在内的其他抗精神病药物相当。PP的耐受性与利培酮相似，最重要的副作用是催乳素升高、体重增加和锥体外系症状。PP的优势包括关于帕利哌酮及其母体化合物利培酮的广泛研究数据库和临床经验、不同长效注射剂型（每月一次、每三个月一次，未来可能还有作用时间更长的剂型）的可获得性，以及无需口服抗精神病药物补充即可快速起效的新型给药起始程序。
