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首页> 外文期刊>Journal of psychopharmacology >Changes in plasma concentrations of risperidone and 9-hydroxyrisperidone and the associated clinical effects during the switch from oral risperidone to extended-release paliperidone tablets in patients with schizophrenia.
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Changes in plasma concentrations of risperidone and 9-hydroxyrisperidone and the associated clinical effects during the switch from oral risperidone to extended-release paliperidone tablets in patients with schizophrenia.

机译：精神分裂症患者从口服利培酮转换为缓释帕潘立酮片期间，利培酮和9-羟基利培酮的血浆浓度变化及相关的临床效果

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This study aimed to investigate changes in plasma concentrations of risperidone and 9-hydroxy-risperidone (9-OHR) and the associated clinical effects when switching from oral risperidone to extended-release (ER) paliperidone in patients with schizophrenia. This study included 25 patients with schizophrenia. Following a one-week screening period with a stable dose of risperidone, a six-week open-label switch study from risperidone to extended-release paliperidone (paliperidone ER) was conducted. Efficacy and safety assessments were performed on Day 1 and at Weeks 1, 2, 4, and 6. Plasma levels of the active fractions of oral risperidone and paliperidone ER were measured on Day 1 and at Week 1, respectively. Plasma levels of the active moiety (risperidone plus 9-OHR) while taking risperidone (mean dose: 4.0 mg) were significantly higher than plasma levels of 9-OHR while taking 6 mg of paliperidone ER. For 12 subjects taking only 3 mg of risperidone, plasma concentrations of the active moiety of risperidone were also significantly higher than those of 9-OHR while taking 6 mg of paliperidone ER. The amount of reduction in plasma levels was correlated with a temporal deterioration of clinical symptoms. These findings suggest that for patients with schizophrenia taking 3 mg or more of risperidone, an initial switching dose of 6 mg of paliperidone ER may be relatively low in terms of subsequent plasma concentrations and the associated clinical response.
机译：这项研究旨在研究精神分裂症患者从口服利培酮转变为缓释帕潘立酮时血浆利培酮和9-羟基-利培酮（9-OHR）的变化以及相关的临床效果。该研究纳入了25例精神分裂症患者。在以稳定剂量的利培酮进行为期一周的筛选后，进行了一项为期六周的从利培酮转向缓释帕潘立酮（帕潘立酮ER）的开放标签转换研究。在第1天和第1、2、4和6周进行功效和安全性评估。分别在第1天和第1周测量口服利培酮和帕潘立酮ER活性成分的血浆水平。服用利培酮（平均剂量：4.0 mg）时活性部分（利培酮加9-OHR）的血浆水平显着高于服用6 mg帕潘立酮ER时的9-OHR血浆水平。对于仅服用3 mg利培酮的受试者，利培酮活性部分的血浆浓度也显着高于9-OHR，而服用6 mg帕潘立酮ER。血浆水平的降低量与临床症状的暂时恶化相关。这些发现表明，对于精神分裂症患者，服用3毫克或更多的利培酮，最初的6毫克帕潘立酮ER的转换剂量在随后的血浆浓度和相关的临床反应方面可能相对较低。

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