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[培氟沙星的临床药理学研究]

[Clinico-pharmacologic studies on pefloxacin].

作者信息

Ludwig E, Székely E, Csiba A

机构信息

Fövárosi Onkormányzat Péterfy Sándor u. Kórház, A Belgyógyászati Osztály és Klinikai Farmakológia, Budapest.

出版信息

Orv Hetil. 1994 Mar 27;135(13):687-92.

PMID:8170669
Abstract

The impact of liver impairment, renal insufficiency and age-related changes on the pharmacokinetics of pefloxacin was studied in 55 patients. The elderly patients were stratified into three age groups (61-70, 71-80 and above 81 years). The patients suffering from various infections were treated with oral or intravenous pefloxacin in a dose of 400 mg bid. Blood samples were withdrawn on the first and seventh day of therapy. The pharmacokinetics of pefloxacin was characterized by marked interindividual differences that became even more pronounced during multiple dosing. The elimination rate of pefloxacin during therapy slowed down, presumably due to its decreased metabolism. In elderly patients, the rate of cumulation is greater than in the young ones, but no significant differences could be detected among the elderly age-groups. Pefloxacin elimination also decreased in renal and hepatic impairment. There was no correlation between serum concentrations of pefloxacin and the development of adverse effects. In elderly subjects and in patients with renal or hepatic impairment, dose reduction might be considered. In mild or moderate infections or in urinary tract infections smaller doses of pefloxacin also could assure good therapeutic results. However, in severe infections especially caused by less susceptible pathogens, routine dose reduction is not recommended because of the significant interindividual differences in serum concentrations of pefloxacin.

摘要

在55例患者中研究了肝功能损害、肾功能不全及年龄相关变化对培氟沙星药代动力学的影响。老年患者被分为三个年龄组(61 - 70岁、71 - 80岁和81岁以上)。患有各种感染的患者接受口服或静脉注射培氟沙星治疗,剂量为400mg,每日两次。在治疗的第一天和第七天采集血样。培氟沙星的药代动力学特征是个体间差异显著,在多次给药期间这种差异更加明显。治疗期间培氟沙星的消除速率减慢,推测是由于其代谢降低。在老年患者中,蓄积率高于年轻患者,但在老年年龄组之间未检测到显著差异。培氟沙星在肝肾功能损害患者中的消除也减少。培氟沙星的血清浓度与不良反应的发生之间没有相关性。对于老年受试者以及肝肾功能损害患者,可能需要考虑减少剂量。在轻度或中度感染或尿路感染中,较小剂量的培氟沙星也可确保良好的治疗效果。然而,在严重感染尤其是由较难敏感病原体引起的感染中,由于培氟沙星血清浓度存在显著个体间差异,不建议常规减少剂量。

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