健康受试者连续口服莫西沙星后其血药浓度与心脏QT间期延长的量变关系评价

发布时间：2018-05-04 19:12

本文选题：莫西沙星 + 血药浓度　；参考：《中国药学杂志》2015年22期

【摘要】：目的在中国健康受试者中评价连续4 d口服给药莫西沙星对健康受试者QT间期的影响。方法筛选48名健康受试者(男女各24名)连续4 d口服400 mg莫西沙星。在给药前、后按预设时间点各描记心电图,使用仪器测量与人工测量方法测定QT间期;同时采集对应时间点的血样,用HPLC-MS/MS进行血药浓度测定;每周期结束时按方案要求进行安全性检查。结果 48名受试者入选本试验,其中45名(男22,女23)完成试验;连续4 d给予莫西沙星口服后可引发QT间期延长7,且给药后血药浓度与QT间期延长的量变关系为正相关,莫西沙星给药后对心脏安全性的危险程度判定为可能危险。结论莫西沙星连续4 d给药可引发有意义与血药浓度正相关的QT间期延长,故建议临床在连续使用莫西沙星时,应结合莫西沙星药代动力学以及QT间期变化的特点,慎重考虑患者尤其是心脏QT间期较长患者的用药。
[Abstract]:Objective to evaluate the effect of oral moxifloxacin on QT interval in Chinese healthy volunteers for 4 days. Methods 48 healthy subjects (24 male and 24 male) were selected to take 400 mg moxifloxacin orally for 4 days. Before and after administration, electrocardiogram was recorded according to preset time points, QT interval was measured by instrument measurement and manual measurement, blood samples of corresponding time points were collected and blood concentration was measured by HPLC-MS/MS. Conduct security checks at the end of each cycle as required by the scheme. Results Forty-eight subjects (22 males and 23 females) completed the trial, and the QT interval was increased by 7 times after oral moxifloxacin for 4 days, and there was a positive correlation between serum concentration and QT interval prolongation after administration of moxifloxacin for 4 days. The risk of cardiac safety after the administration of moxifloxacin was determined to be potentially dangerous. Conclusion moxifloxacin administration for 4 days can induce significant prolongation of QT interval which is positively correlated with serum concentration. It is suggested that moxifloxacin pharmacokinetics and QT interval change should be combined with the clinical use of moxifloxacin continuously. Consider carefully the use of drugs in patients, especially in patients with longer QT intervals in the heart.
【作者单位】：解放军总医院转化医学中心;
【基金】：国家科技重大专项子课题资助项目(2012ZX09303004-002)
【分类号】：R969.4

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