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抗精神病药物利培酮的QT间期延长主要与其9-羟基代谢物帕利哌酮有关。

QT prolongation of the antipsychotic risperidone is predominantly related to its 9-hydroxy metabolite paliperidone.

作者信息

Suzuki Yutaro, Fukui Naoki, Watanabe Junzo, Ono Shin, Sugai Takuro, Tsuneyama Nobuto, Saito Mami, Inoue Yoshimasa, Someya Toshiyuki

机构信息

Department of Psychiatry, Niigata University Graduate School of Medical and Dental Sciences, Niigata, Japan.

出版信息

Hum Psychopharmacol. 2012 Jan;27(1):39-42. doi: 10.1002/hup.1258. Epub 2011 Dec 5.

DOI:10.1002/hup.1258
PMID:22144033
Abstract

OBJECTIVE

A dose-dependent increase in risk of sudden cardiac death for the antipsychotic drug risperidone was reported. However, few reports have so far addressed QT prolongation associated with the use of risperidone or its major active metabolite, which is also used as a separate antipsychotic drug, paliperidone.

METHODS

The present study evaluated associations between risperidone metabolism and QT interval in 61 psychiatric patients who had been receiving risperidone for ≥4 weeks at an average dosage of 4.7 mg/day. Plasma risperidone and paliperidone levels were measured and electrocardiographic measurements were also obtained.

RESULTS

There was no correlation between risperidone dosage and QTc or plasma risperidone levels and QTc. However, there was a significant positive correlation between plasma paliperidone levels and QTc (r = 0.361; p = 0.004). There was no correlation between age and dose-corrected plasma risperidone levels or between age and QTc. There was a significant positive correlation between age and dose-corrected plasma paliperidone levels (r = 0.290; p = 0.023).

CONCLUSION

Clinically, paliperidone is considered to play a more important role in QT prolongation than risperidone.

摘要

目的

有报道称抗精神病药物利培酮会使心脏性猝死风险呈剂量依赖性增加。然而,迄今为止,很少有报告涉及与利培酮或其主要活性代谢产物(该代谢产物也作为一种单独的抗精神病药物帕利哌酮使用)使用相关的QT间期延长问题。

方法

本研究评估了61例接受利培酮治疗≥4周、平均剂量为4.7毫克/天的精神科患者中利培酮代谢与QT间期之间的关联。测量了血浆利培酮和帕利哌酮水平,并进行了心电图测量。

结果

利培酮剂量与QTc之间、血浆利培酮水平与QTc之间均无相关性。然而,血浆帕利哌酮水平与QTc之间存在显著正相关(r = 0.361;p = 0.004)。年龄与剂量校正后的血浆利培酮水平之间、年龄与QTc之间均无相关性。年龄与剂量校正后的血浆帕利哌酮水平之间存在显著正相关(r = 0.290;p = 0.023)。

结论

临床上,帕利哌酮在QT间期延长方面被认为比利培酮发挥着更重要的作用。

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