Abgueguen Pierre, Azoulay-Dupuis Esther, Noel Violaine, Moine Pierre, Rieux Veronique, Fantin Bruno, Bedos Jean-Pierre
Service des Maladies Infectieuses et Tropicales, Centre Hospitalier Universitaire d'Angers, 4 rue Larrey, 49933 Angers Cedex 9, France.
Antimicrob Agents Chemother. 2007 Jan;51(1):208-14. doi: 10.1128/AAC.00004-06. Epub 2006 Oct 23.
High-dose oral amoxicillin (3 g/day) is the recommended empirical outpatient treatment of community-acquired pneumonia (CAP) in many European guidelines. To investigate the clinical efficacy of this treatment in CAP caused by Streptococcus pneumoniae strains with MICs of amoxicillin > or =2 microg/ml, we used a lethal bacteremic pneumonia model in leukopenic female Swiss mice with induced renal failure to replicate amoxicillin kinetics in humans given 1 g/8 h orally. Amoxicillin (15 mg/kg of body weight/8 h subcutaneously) was given for 3 days. We used four S. pneumoniae strains with differing amoxicillin susceptibility and tolerance profiles. Rapid bacterial killing occurred with an amoxicillin-susceptible nontolerant strain: after 4 h, blood cultures were negative and lung homogenate counts under the 2 log(10) CFU/ml detection threshold (6.5 log(10) CFU/ml in controls, P < 0.01). With an amoxicillin-intermediate nontolerant strain, significant pulmonary bacterial clearance was observed after 24 h (4.3 versus 7.9 log(10) CFU/ml, P < 0.01), and counts were undetectable 12 h after treatment completion. With an amoxicillin-intermediate tolerant strain, 24-h bacterial clearance was similar (5.4 versus 8.3 log(10) CFU/ml, P < 0.05), but 12 h after treatment completion, lung homogenates contained 3.3 log(10) CFU/ml. Similar results were obtained with an amoxicillin-resistant and -tolerant strain. Day 10 survival rates were usually similar across strains. Amoxicillin with pharmacokinetics simulating 1 g/8 h orally in humans is bactericidal in mice with pneumonia due to S. pneumoniae for which MICs were 2 to 4 microg/ml. The killing rate depends not only on resistance but also on tolerance of the S. pneumoniae strains.
在许多欧洲指南中,高剂量口服阿莫西林(3克/天)是社区获得性肺炎(CAP)推荐的经验性门诊治疗方法。为研究这种治疗方法对阿莫西林最低抑菌浓度(MIC)≥2微克/毫升的肺炎链球菌菌株所致CAP的临床疗效,我们在患有诱导性肾衰竭的白细胞减少雌性瑞士小鼠中使用致死性菌血症肺炎模型,以模拟人类口服1克/8小时后阿莫西林的动力学。皮下注射阿莫西林(15毫克/千克体重/8小时),持续3天。我们使用了4株对阿莫西林敏感性和耐受性不同的肺炎链球菌菌株。对于一株对阿莫西林敏感且无耐受性的菌株,细菌迅速被杀灭:4小时后,血培养呈阴性,肺匀浆菌落计数低于2 log(10) CFU/毫升的检测阈值(对照组为6.5 log(10) CFU/毫升,P < 0.01)。对于一株对阿莫西林中度敏感且无耐受性的菌株,24小时后观察到显著的肺部细菌清除(4.3对7.9 log(10) CFU/毫升,P < 0.01),治疗结束后12小时菌落计数无法检测到。对于一株对阿莫西林中度敏感且有耐受性的菌株,24小时细菌清除情况相似(5.4对8.3 log(10) CFU/毫升,P < 0.05),但治疗结束后12小时,肺匀浆中含有3.3 log(10) CFU/毫升。一株对阿莫西林耐药且有耐受性的菌株也得到了类似结果。不同菌株第10天的生存率通常相似。在人类中模拟口服1克/8小时药代动力学的阿莫西林对肺炎链球菌所致肺炎的小鼠具有杀菌作用,这些肺炎链球菌的MIC为2至4微克/毫升。杀灭率不仅取决于肺炎链球菌菌株的耐药性,还取决于其耐受性。