Wijnands W J, Vree T B, Van Herwaarden C L
Pharm Weekbl Sci. 1986 Feb 21;8(1):42-5. doi: 10.1007/BF01975479.
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.
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。
