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4-喹诺酮类药物依诺沙星对血浆茶碱浓度的影响。

The effect of the 4-quinolone enoxacin on plasma theophylline concentrations.

作者信息

Wijnands W J, Vree T B, Van Herwaarden C L

出版信息

Pharm Weekbl Sci. 1986 Feb 21;8(1):42-5. doi: 10.1007/BF01975479.

Abstract

In patients treated concomitantly with theophylline and enoxacin, a broad spectrum antibacterial agent for oral administration, unexpectedly high plasma theophylline concentrations were observed. In six patients receiving intravenous aminophylline under controlled conditions, enoxacin was started in a daily dose of 800 or 1200 mg. Plasma theophylline concentrations increased from 8.4 +/- 2.4 mg/l to 15.0 +/- 5.1 mg/l at day 3 of co-administration. Total body clearance of theophylline decreased significantly, whereas renal clearance and protein binding did not change. When enoxacin, 800 mg daily, was administered to seven patients with a stable chronic obstructive pulmonary disease, who were on long-term theophylline treatment a significant increase in plasma theophylline concentrations occurred as well: elimination half-life was prolonged. It is concluded that the rise of plasma theophylline concentrations is caused by a reduced metabolic clearance of theophylline. If concomitant use of both drugs is necessary, monitoring of plasma theophylline concentration and adjustment of the theophylline dose is recommended, to avoid toxicity.

摘要

在同时接受茶碱和口服广谱抗菌剂依诺沙星治疗的患者中,观察到血浆茶碱浓度意外升高。在6名在受控条件下接受静脉注射氨茶碱的患者中,开始每日服用800或1200毫克依诺沙星。联合用药第3天时,血浆茶碱浓度从8.4±2.4毫克/升增至15.0±5.1毫克/升。茶碱的总体清除率显著降低,而肾清除率和蛋白结合率未改变。当对7名长期接受茶碱治疗的稳定型慢性阻塞性肺疾病患者每日给予800毫克依诺沙星时,血浆茶碱浓度也显著升高:消除半衰期延长。得出的结论是,血浆茶碱浓度升高是由茶碱代谢清除率降低所致。如果必须同时使用这两种药物,建议监测血浆茶碱浓度并调整茶碱剂量,以避免毒性。

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