Penetration of Levofloxacin into Lung Tissue after Oral Administration to Subjects Undergoing Lung Biopsy or Lobectomy

Abstract

Study Objective. To evaluate the pulmonary tissue distribution of levofloxacin, the new once‐daily fluoroquinolone, after a single 500‐mg oral dose.Design. Open‐label study.Setting. One pulmonary clinic and two university‐affiliated teaching hospitals.Patients. Eighteen adults undergoing lung biopsy or lobectomy.Interventions. Levofloxacin plasma and lung tissue concentrations were determined by high‐performance liquid chromatography with fluorescence detection. Lung tissue levofloxacin concentrations were corrected for blood contamination by measuring hemoglobin.Measurements and Main Results. After a single 500‐mg oral dose, concentrations of levofloxacin in lung tissue consistently exceeded those in plasma at every time point over the 24‐hour sampling period, with tissue:plasma penetration ratios of 2.02 (2–3 hrs), 5.02 (4–6 hrs), 5.13 (11–17 hrs), and 4.13 (22–25 hrs). The mean penetration ratio over the 24‐hour sampling period was 3.95 (range 1.06–9.98). Lung tissue concentrations of levofloxacin also exceeded minimum inhibitory concentration values for most community‐acquired respiratory tract pathogens over the 24 hours.Conclusion. This study supports clinical evaluation of levofloxacin as once‐daily oral therapy for community‐acquired lower respiratory tract infections.