Wijnands W J, Vree T B, Van Herwaarden C L
Br J Clin Pharmacol. 1985 Dec;20(6):583-8. doi: 10.1111/j.1365-2125.1985.tb05115.x.
In patients treated concurrently with theophylline and enoxacin, a new broad-spectrum antibacterial agent of the quinolone class, unexpectedly high plasma theophylline concentrations were measured. In part I of this study, daily plasma theophylline concentrations were measured in 14 patients. The mean +/- s.d. theophylline concentrations increased from 8.5 +/- 2.8 micrograms ml-1 prior to enoxacin to a maximum of 21.7 +/- 7.8 micrograms ml-1 during coadministration. In part II, six of these patients received aminophylline intravenously at a constant infusion rate and under controlled conditions. Plasma theophylline concentrations rose from 8.4 +/- 2.4 micrograms ml-1 prior to enoxacin treatment to 15.0 +/- 5.1 micrograms ml-1 at day 3 of coadministration (P less than 0.005). Plasma protein-binding and renal clearance of theophylline remained unchanged, whereas total body clearance of theophylline significantly decreased (P less than 0.005). From these observations 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.
在同时接受茶碱和新的喹诺酮类广谱抗菌药依诺沙星治疗的患者中,测得血浆茶碱浓度意外地高。在本研究的第一部分,对14例患者每日测定血浆茶碱浓度。茶碱浓度的均值±标准差从依诺沙星治疗前的8.5±2.8微克/毫升增加到联合用药期间的最高值21.7±7.8微克/毫升。在第二部分,其中6例患者在控制条件下以恒定输注速率静脉给予氨茶碱。血浆茶碱浓度从依诺沙星治疗前的8.4±2.4微克/毫升升至联合用药第3天的15.0±5.1微克/毫升(P<0.005)。茶碱的血浆蛋白结合率和肾清除率保持不变,而茶碱的总体清除率显著降低(P<0.005)。从这些观察结果得出结论,血浆茶碱浓度的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。