Cesana M, Broccali G, Imbimbo B P, Crema A
Medical Department, Mediolanum Farmaceutici, Milan, Italy.
Int J Clin Pharmacol Ther Toxicol. 1991 Apr;29(4):133-8.
Several reports indicate that quinolone antibiotics affect the pharmacokinetics of theophylline and caffeine. This study investigated the effects of one single oral dose of rufloxacin, a new quinolone antibacterial, on the pharmacokinetics of theophylline and caffeine, given as single oral doses. Twelve healthy male volunteers were randomly given one of the following treatments: treatment T: 300 mg theophylline; treatment T + R: 300 mg theophylline followed by 400 mg rufloxacin after 30 min; treatment C: 200 mg caffeine; treatment C + R: 200 mg caffeine followed by 400 mg rufloxacin after 30 min. Blood samples for determination of xanthine plasma levels were taken immediately before and 1, 2, 4, 6, 8, 10, 12, 24 and 48 hours after xanthine administration. Urine were collected before treatment and at 0-6, 6-12, 12-24 and 24-48 h intervals. There were no significant differences in the pharmacokinetic parameters or in urinary excretion after administration of either theophylline or caffeine when combined with rufloxacin. Sleep disturbances were reported by two subjects after both treatment T + R and C + R, and by four subjects after treatment T + R. The results of this study indicate that there is no significant pharmacokinetic interaction between a single oral dose of rufloxacin and single doses of theophylline and caffeine.
几份报告表明喹诺酮类抗生素会影响茶碱和咖啡因的药代动力学。本研究调查了单次口服新型喹诺酮类抗菌药物芦氟沙星对单次口服给药的茶碱和咖啡因药代动力学的影响。12名健康男性志愿者被随机给予以下治疗之一：治疗T：300mg茶碱；治疗T + R：300mg茶碱，30分钟后服用400mg芦氟沙星；治疗C：200mg咖啡因；治疗C + R：200mg咖啡因，30分钟后服用400mg芦氟沙星。在给予黄嘌呤前以及给药后1、2、4、6、8、10、12、24和48小时采集血样以测定血浆黄嘌呤水平。在治疗前以及0 - 6、6 - 12、12 - 24和24 - 48小时间隔收集尿液。当茶碱或咖啡因与芦氟沙星合用时，其药代动力学参数或尿排泄没有显著差异。在治疗T + R和C + R后，有两名受试者报告了睡眠障碍，在治疗T + R后有四名受试者报告了睡眠障碍。本研究结果表明，单次口服芦氟沙星与单次口服茶碱和咖啡因之间不存在显著的药代动力学相互作用。
