Weinrich Malte, Scheingraber Stefan, Stremovskaia Tatiana, Schilling Martin K, Kees Frieder, Pistorius Georg A
Department of General, Visceral, Vascular and Pediatric Surgery, University Hospital of the Saarland, Kirrberger Strasse, D-66421 Homburg/Saar, Germany.
Int J Antimicrob Agents. 2006 Sep;28(3):221-5. doi: 10.1016/j.ijantimicag.2006.04.012. Epub 2006 Aug 14.
High concentrations of levofloxacin in soft tissues and body fluids, including gallbladder and bile, have been repeatedly reported, but no study on its penetration into human liver tissue after single-shot application has yet been published. Levofloxacin 500 mg was administered intravenously to 28 patients scheduled for liver resection. Blood samples were taken after the end of infusion and at the time of liver resection; concomitantly, a tissue specimen was also obtained. Serum concentrations (mean+/-standard deviation) 10 min after the end of infusion were 6.59+/-1.72 microg/mL and decreased only slightly throughout the operation. At the time of liver resection, levofloxacin concentrations in liver tissue were 18.14+/-5.44 microg/g with corresponding serum concentrations of 4.84+/-1.37 microg/mL. The tissue/serum ratio (3.72+/-0.73 at the time of resection) was nearly constant over the sampling period ranging from 0.4 h to 3.8 h after the end of infusion, indicating a fast distribution of levofloxacin into the liver tissue. The tissue concentrations showed a significant correlation with serum concentrations and an inverse correlation with the grade of steatosis but not cirrhosis. Infectious post-operative complications were not observed. Levofloxacin penetrates into liver tissue exceptionally well and fast and is therefore a good candidate for antibiotic prophylaxis before invasive hepatobiliary procedures such as liver surgery as well as for treatment of biliary tract infections caused by levofloxacin-susceptible microorganisms.
已有多次报道称，左氧氟沙星在包括胆囊和胆汁在内的软组织和体液中浓度较高，但单次给药后其在人体肝组织中的渗透情况尚无相关研究发表。对28例计划进行肝切除术的患者静脉注射500mg左氧氟沙星。输液结束后及肝切除时采集血样；同时，还获取了一份组织标本。输液结束10分钟后的血清浓度（平均值±标准差）为6.59±1.72μg/mL，且在整个手术过程中仅略有下降。肝切除时，肝组织中的左氧氟沙星浓度为18.14±5.44μg/g，相应的血清浓度为4.84±1.37μg/mL。组织/血清比值（切除时为3.72±0.73）在输液结束后0.4小时至3.8小时的采样期内几乎保持恒定，表明左氧氟沙星能快速分布到肝组织中。组织浓度与血清浓度呈显著正相关，与脂肪变性程度呈负相关，但与肝硬化无关。未观察到术后感染并发症。左氧氟沙星能异常快速地渗透到肝组织中，因此是侵入性肝胆手术（如肝手术）前抗生素预防以及治疗由左氧氟沙星敏感微生物引起的胆道感染的良好选择。
