Adis, a Wolters Kluwer Business, Auckland, New Zealand.
CNS Drugs. 2010 Mar;24(3):227-44. doi: 10.2165/11203810-000000000-00000.
Intramuscular paliperidone palmitate is a long-acting, atypical antipsychotic that is indicated in the US for the acute and maintenance therapy of adult patients with schizophrenia. Paliperidone is the major active metabolite of risperidone. The noninferiority of flexible doses of intramuscular paliperidone palmitate 39-156 mg to flexible doses of intramuscular long-acting risperidone 25-50 mg was not established in an initial 53-week study. However, these data were utilized to optimize the intramuscular paliperidone palmitate dosage regimen. In four randomized, double-blind studies, intramuscular paliperidone palmitate 39-234 mg was generally effective in the treatment of adult patients with acute schizophrenia, inducing significantly greater improvements from baseline in the mean Positive and Negative Syndrome Scale (PANSS) total score than placebo (primary endpoint). In general, intramuscular paliperidone palmitate recipients achieved significantly better outcomes than placebo recipients with regard to the PANSS subscale, PANSS factor, Personal and Social Performance scale and Clinical Global Impressions-Severity scale scores. As maintenance therapy, intramuscular paliperidone palmitate 39-156 mg was significantly more effective than placebo in delaying the time to the first relapse of schizophrenia symptoms in adult patients, according to the results of a randomized, double-blind study. The beneficial effects of intramuscular paliperidone palmitate therapy on the PANSS total score were sustained in a 52-week noncomparative extension phase of the maintenance therapy study. Intramuscular paliperidone palmitate 39-234 mg was generally well tolerated in adult patients with schizophrenia.
棕榈酸帕利哌酮注射液是一种长效非典型抗精神病药，于美国获批用于成人精神分裂症患者的急性期和维持期治疗。帕利哌酮是利培酮的主要活性代谢物。在一项最初为期 53 周的研究中，并未确立灵活剂量的肌肉注射棕榈酸帕利哌酮 39-156mg 与灵活剂量的肌肉注射长效利培酮 25-50mg 的非劣效性。然而，这些数据被用于优化肌肉注射棕榈酸帕利哌酮的剂量方案。在四项随机、双盲研究中，肌肉注射棕榈酸帕利哌酮 39-234mg 通常可有效治疗急性精神分裂症成人患者，与安慰剂相比，从基线水平显著改善阳性和阴性综合征量表（PANSS）总分（主要终点）。一般来说，与安慰剂组相比，肌肉注射棕榈酸帕利哌酮组在 PANSS 子量表、PANSS 因子、个人和社会表现量表和临床总体印象-严重度量表评分方面的结局显著更好。作为维持治疗，在一项随机、双盲研究中，与安慰剂相比，肌肉注射棕榈酸帕利哌酮 39-156mg 可显著延迟精神分裂症症状首次复发的时间，从而使成人患者获益。维持治疗研究的 52 周非比较扩展阶段的结果表明，肌肉注射棕榈酸帕利哌酮治疗对 PANSS 总分的有益作用得以持续。肌肉注射棕榈酸帕利哌酮 39-234mg 通常在精神分裂症成年患者中具有良好的耐受性。
