LeBel M, Bergeron M G, Vallée F, Fiset C, Chassé G, Bigonesse P, Rivard G
Antimicrob Agents Chemother. 1986 Aug;30(2):260-6. doi: 10.1128/AAC.30.2.260.
The pharmacokinetics and blister fluid penetration of oral ciprofloxacin were compared in 11 cystic fibrosis (CF) patients who had sputum colonization but were asymptomatic and in 12 healthy volunteers after a single dose (500 mg) and at steady state (500 mg every 8 h). The antibacterial effect of ciprofloxacin therapy was also evaluated by bacterial counts of colonizing pathogens in the respiratory secretions of CF patients. The CF patients were 15.9% lighter in weight than the controls (P less than 0.05). After a single dose, the elimination half-life of ciprofloxacin was decreased by a third in the CF patients as compared with the controls (2.62 versus 3.93 h, respectively; P less than 0.01). This was the result of a diminished apparent volume of distribution in CF subjects. Interestingly, we observed no statistically significant difference in total apparent and renal clearances between the groups. Suction-induced blister fluid penetration was not different between CF patients and healthy volunteers. In CF patients, ciprofloxacin exhibited levels in respiratory secretions above the reported MIC for Pseudomonas aeruginosa: 1.36 and 1.86 micrograms/ml at 2 h after a single dose and at steady state, respectively. An important fall (mean, 3.9 log10/ml) in the log titer in 10 patients with P. aeruginosa in their respiratory secretions was observed after 5 days of treatment. However, this improvement was short-lived; the secondary increase in bacterial counts observed in five patients and the development of five resistant strains were causes for concern. The pharmacokinetic results presented here showed that ciprofloxacin should be administered every 8 or even every 6 h in CF patients.
对11名痰菌定植但无症状的囊性纤维化(CF)患者和12名健康志愿者,比较了单剂量(500mg)及稳态(每8小时500mg)口服环丙沙星后的药代动力学及水疱液渗透情况。还通过CF患者呼吸道分泌物中定植病原体的细菌计数评估了环丙沙星治疗的抗菌效果。CF患者体重比对照组轻15.9%(P<0.05)。单剂量给药后,CF患者中环丙沙星的消除半衰期比对照组缩短了三分之一(分别为2.62小时和3.93小时;P<0.01)。这是CF受试者表观分布容积减小的结果。有趣的是,我们观察到两组之间的总表观清除率和肾清除率无统计学显著差异。CF患者和健康志愿者之间的抽吸诱导水疱液渗透情况无差异。在CF患者中,环丙沙星在呼吸道分泌物中的水平高于报道的铜绿假单胞菌最低抑菌浓度:单剂量给药后2小时及稳态时分别为1.36和1.86μg/ml。治疗5天后,观察到10名呼吸道分泌物中有铜绿假单胞菌的患者的对数滴度有显著下降(平均3.9 log10/ml)。然而,这种改善是短暂的;5名患者细菌计数的二次增加以及5株耐药菌株的出现令人担忧。此处呈现的药代动力学结果表明,CF患者中环丙沙星应每8小时甚至每6小时给药一次。