Department of Psychiatry, Neurochemical Research Unit, University of Alberta, Edmonton, Alberta, Canada.
Expert Rev Neurother. 2012 Dec;12(12):1399-410. doi: 10.1586/ern.12.138.
Paliperidone, or 9-hydroxyrisperidone (Invega(®), Janssen, Antwerp, Belgium) is the major active metabolite of the atypical antipsychotic risperidone (Risperdal(®), Janssen). It possesses a similar, though not identical, receptor pharmacology to the parent molecule. There are additional differences in terms of its predominant renal metabolism, lower protein binding and decreased inhibition of P-glycoprotein leading to decreased potential for drug-drug interactions. Paliperidone is approved as an extended release (ER) tablet based on an osmotic-controlled release oral Push-Pull™ delivery system (Oral Osmotic System, OROS(®), Alza Corporation) for the treatment of schizophrenia. The ER formulation results in decreased fluctuations in plasma drug levels and allows for once-daily administration with initial tolerability that permits treatment initiation at a clinically effective dose without the need for titration. This achieves therapeutic levels rapidly and simplifies dosing regimens, leading to potentially better adherence and improved outcome. The present review focuses on the clinical implications of the pharmacology and formulation of paliperidone ER.
帕利哌酮，或 9-羟基利培酮（商品名：善思达，杨森制药，比利时安特卫普），是一种非典型抗精神病药物利培酮（商品名：芮达，杨森制药）的主要活性代谢产物。它具有与母体分子相似但不完全相同的受体药理学特性。在其主要的肾脏代谢、较低的蛋白结合率和对 P 糖蛋白的抑制作用降低方面存在额外的差异，从而降低了药物相互作用的潜力。帕利哌酮基于一种渗透压控制的释放口服推-拉式（Oral Push-Pull）输送系统（Oral Osmotic System，OROS®，Alza 公司），被批准为一种延长释放（ER）片剂，用于治疗精神分裂症。ER 制剂可降低血浆药物水平的波动，允许每日一次给药，初始耐受性好，可在临床有效剂量下开始治疗，无需滴定。这可迅速达到治疗水平并简化给药方案，从而可能提高患者的依从性和改善治疗结果。本综述重点关注帕利哌酮 ER 的药理学和制剂学的临床意义。
