Macaluso Matthew, Oliver Hannah, Sohail Zohaib
a Psychiatry and Behavioral Sciences , University of Kansas School of Medicine , Wichita , KS , USA.
Expert Opin Drug Metab Toxicol. 2017 Aug;13(8):871-879. doi: 10.1080/17425255.2017.1351546. Epub 2017 Jul 12.
This paper reviews the pharmacokinetics, receptor binding, clinical efficacy and safety of paliperidone in the treatment of patients with schizoaffective disorder. Areas covered: We reviewed the literature using keywords 'paliperidone', 'schizoaffective disorder' and 'clinical trials' with a focus on seminal data papers and information that is clinically relevant to the treatment of schizoaffective disorder. The purpose of this paper is to provide a clinically oriented review of the pharmacokinetic and pharmacodynamic properties of paliperidone including receptor binding, clinical efficacy, safety and tolerability. Expert opinion: Paliperidone is currently the only medication FDA approved specifically for the treatment of schizoaffective disorder. Paliperidone is an active metabolite of risperidone, is minimally metabolized in the liver and is primarily known to be cleared through the kidneys. For this reason, paliperidone could be considered for some patients with schizoaffective disorder who also have hepatic impairment. After correcting for the reduced protein binding that is characteristic of hepatically impaired patients, the Cmax was 12% lower than in healthy subjects while the AUC and CL/F were comparable [14]. In addition, the availability of long acting injectable formulations may be useful for patients who are non-adherent with oral medications. The cost of paliperidone may be a disadvantage.
本文综述了帕利哌酮治疗分裂情感性障碍患者的药代动力学、受体结合情况、临床疗效及安全性。涵盖领域:我们使用关键词“帕利哌酮”“分裂情感性障碍”和“临床试验”检索文献,重点关注关键数据论文以及与分裂情感性障碍治疗临床相关的信息。本文旨在对帕利哌酮的药代动力学和药效学特性进行以临床为导向的综述,包括受体结合、临床疗效、安全性和耐受性。专家观点:帕利哌酮是目前美国食品药品监督管理局(FDA)唯一批准专门用于治疗分裂情感性障碍的药物。帕利哌酮是利培酮的活性代谢产物,在肝脏中代谢极少,主要通过肾脏清除。因此,对于一些同时患有肝损伤的分裂情感性障碍患者,可以考虑使用帕利哌酮。在纠正了肝损伤患者特有的蛋白结合降低情况后,其Cmax比健康受试者低12%,而AUC和CL/F相当[14]。此外,长效注射制剂的可用性可能对不依从口服药物治疗的患者有用。帕利哌酮的费用可能是一个劣势。