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肝硬化患者中氟西汀的清除率。

Femoxetine clearance in patients with liver cirrhosis.

作者信息

Hansen B A, Mengel H, Keiding S, Lund J

出版信息

Acta Pharmacol Toxicol (Copenh). 1984 Nov;55(5):386-90. doi: 10.1111/j.1600-0773.1984.tb01999.x.

Abstract

The pharmacokinetics of femoxetine (a 5-HT uptake inhibitor with antidepressive effect) was studied in 12 patients with liver cirrhosis and in 6 healthy controls after a single oral dose of femoxetine HC1. The average blood concentration of femoxetine, as assessed by the values of AUC (area under the plasma concentration/time curve), was significantly higher in the patients with liver cirrhosis than in the healthy controls in spite of dose reduction in the patients. The elimination half-life of femoxetine was within the normal limits in most of the patients. The oral clearance of femoxetine was considerably lower in patients, (0.65-4.02 1/hr/kg) than in the controls (8.13- greater than 50 1/hr/kg). It was not directly related to the metabolic function of the liver, measured as the galactose elimination capacity being 0.015-0.024 mmol/min./kg and 0.033-0.041 mmol/min./kg, respectively. When treating patients with reduced liver function, it is recommended to reduce the doses and to monitor closely the plasma levels.

摘要

在12例肝硬化患者和6例健康对照者中,单次口服盐酸非莫西汀(一种具有抗抑郁作用的5-羟色胺摄取抑制剂)后,对其药代动力学进行了研究。尽管患者剂量有所减少,但通过AUC(血浆浓度/时间曲线下面积)值评估,肝硬化患者中非莫西汀的平均血药浓度显著高于健康对照者。大多数患者中非莫西汀的消除半衰期在正常范围内。患者中非莫西汀的口服清除率(0.65 - 4.02升/小时/千克)显著低于对照者(8.13 - 大于50升/小时/千克)。它与肝脏的代谢功能没有直接关系,肝脏代谢功能分别通过半乳糖清除能力来衡量,肝硬化患者为0.015 - 0.024毫摩尔/分钟/千克,健康对照者为0.033 - 0.041毫摩尔/分钟/千克。治疗肝功能减退的患者时,建议减少剂量并密切监测血浆水平。

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