Johnson & Johnson Pharmaceutical Research and Development, Titusville, NJ 08560, USA.
J Psychopharmacol. 2010 Jul;24(7):1011-8. doi: 10.1177/0269881109106914. Epub 2009 Oct 13.
Increases in serum prolactin concentrations after administration of risperidone have been attributed, by some, to the availability of paliperidone in plasma. This double-blind, randomized, parallel-group study in patients with schizophrenia compared serum prolactin concentrations following the administration of paliperidone extended-release and risperidone immediate-release tablets. At steady state, the doses administered resulted in a similar exposure to paliperidone and the pharmacologically active fraction of risperidone (i.e. risperidone + paliperidone), respectively. Eligible patients were randomized to either paliperidone extended-release 12 mg on days 1-6 or risperidone immediate-release 2 mg on day 1 and 4 mg on days 2-6. Mean serum prolactin concentrations increased on day 1 (C(max): 71.8 ng/ml and 89.7 ng/ml reached at 6.5 hours and 2.6 hours for paliperidone extended-release and risperidone immediate-release, respectively). On day 6, serum prolactin concentration-time profiles were similar for both treatments, with overall higher serum prolactin concentrations than on day 1 (AUC(0-24 h): 1389 and 842 ng h/ml, and 1306 and 741 ng.h/ml on day 6 and day 1 for paliperidone extended-release and risperidone immediate-release, respectively). These results indicate that paliperidone extended-release 12 mg and risperidone immediate-release 4 mg, administered over a period of 6 days, lead to similar elevations in serum prolactin concentrations.
在一些研究中，利培酮治疗后血清催乳素浓度的增加归因于帕利哌酮在血浆中的可用性。这项双盲、随机、平行组研究比较了精神分裂症患者在服用帕利哌酮长效和利培酮速释片后血清催乳素浓度的变化。在稳态时，所给予的剂量导致帕利哌酮和利培酮的药理活性部分（即利培酮+帕利哌酮）分别具有相似的暴露量。符合条件的患者被随机分为帕利哌酮长效 12 mg 组（第 1-6 天）或利培酮速释 2 mg 组（第 1 天）和 4 mg 组（第 2-6 天）。第 1 天，血清催乳素浓度升高（C(max)：帕利哌酮长效和利培酮速释分别为 71.8ng/ml 和 89.7ng/ml，分别在 6.5 小时和 2.6 小时达到）。第 6 天，两种治疗方法的血清催乳素浓度-时间曲线相似，总血清催乳素浓度均高于第 1 天（AUC(0-24 h)：帕利哌酮长效和利培酮速释分别为 1389 和 842ng.h/ml，以及 1306 和 741ng.h/ml）。这些结果表明，帕利哌酮长效 12 mg 和利培酮速释 4 mg 在 6 天内给药，导致血清催乳素浓度相似升高。
