Baldwin D R, Andrews J M, Wise R, Honeybourne D
Department of Thoracic Medicine, Dudley Road Hospital, Birmingham, UK.
J Antimicrob Chemother. 1992 Sep;30(3):377-85. doi: 10.1093/jac/30.3.377.
The concentrations of cefuroxime in human alveolar macrophages (AM), epithelial lining fluid (ELF), bronchial mucosal biopsies and serum were measured after a single dose, equivalent to 500 mg of cefuroxime base, given in the form of the orally-administered pro-drug, cefuroxime axetil. Fourteen patients undergoing fibreoptic bronchoscopy with bronchoalveolar lavage were studied. The mean ELF concentration was 0.7 mg/L, that of bronchial biopsies was 1.8 mg/kg and that of serum 3.5 mg/L. AM-associated cefuroxime was detected in nine patients. To assess the in-vitro activity of the concentrations achieved at the potential sites of infection, clinical isolates of common respiratory pathogens were exposed to two concentrations of cefuroxime, based on the observed concentrations in ELF and bronchial mucosa. ELF and mucosal site concentrations were effective against Streptococcus pneumoniae (except one strain with reduced susceptibility to benzyl penicillin) and Haemophilus influenzae. The ELF concentration was less effective against Moraxella catarrhalis.
以口服前体药物头孢呋辛酯的形式给予相当于500mg头孢呋辛碱基的单剂量药物后，测定了人肺泡巨噬细胞（AM）、上皮衬液（ELF）、支气管黏膜活检组织和血清中头孢呋辛的浓度。研究了14例接受纤维支气管镜检查并进行支气管肺泡灌洗的患者。ELF的平均浓度为0.7mg/L，支气管活检组织的平均浓度为1.8mg/kg，血清的平均浓度为3.5mg/L。在9例患者中检测到与AM相关的头孢呋辛。为了评估在潜在感染部位所达到的浓度的体外活性，根据在ELF和支气管黏膜中观察到的浓度，将常见呼吸道病原体的临床分离株暴露于两种浓度的头孢呋辛中。ELF和黏膜部位的浓度对肺炎链球菌（除一株对苄青霉素敏感性降低的菌株外）和流感嗜血杆菌有效。ELF浓度对卡他莫拉菌的效果较差。
