Grayo Solène, Lott-Desroches Marie-Catherine, Dussurget Olivier, Respaud Renaud, Fontanet Arnaud, Join-Lambert Olivier, Singlas Eric, Le Monnier Alban
Laboratoire de Listeria, Centre National de Référence des Listeria, World Health Organization Collaborating Centre for Foodborne Listeriosis, Institut Pasteur, Paris, France.
Antimicrob Agents Chemother. 2008 Sep;52(9):3210-5. doi: 10.1128/AAC.00177-08. Epub 2008 Jun 23.
Listeriosis is a rare but life-threatening infection. A favorable outcome is greatly aided by early administration of antibiotics with rapid bactericidal activity against Listeria monocytogenes. Moxifloxacin, a new-generation fluoroquinolone with extended activity against gram-positive bacteria, has proved its effectiveness in vitro against intracellular reservoirs of bacteria. The efficacies of moxifloxacin and amoxicillin were compared in vivo by survival curve assays and by studying the kinetics of bacterial growth in blood and organs in a murine model of central nervous system (CNS) listeriosis. We combined pharmacokinetic and pharmacodynamic approaches to correlate the observed efficacy in vivo with plasma and tissue moxifloxacin concentrations. Death was significantly delayed for animals treated with a single dose of moxifloxacin compared to a single dose of amoxicillin. We observed rapid bacterial clearance from blood and organs of animals treated with moxifloxacin. The decrease in the bacterial counts in blood and brain correlated with plasma and cerebral concentrations of antibiotic. Moxifloxacin peaked in the brain at 1.92 +/- 0.32 microg/g 1 hour after intraperitoneal injection. This suggests that moxifloxacin rapidly crosses the blood-brain barrier and diffuses into the cerebral parenchyma. Moreover, no resistant strains were selected during in vivo experiments. Our results indicate that moxifloxacin combines useful pharmacokinetic properties and rapid bactericidal activity and that it may be a valuable alternative for the treatment of CNS listeriosis.
李斯特菌病是一种罕见但危及生命的感染。早期使用对单核细胞增生李斯特菌具有快速杀菌活性的抗生素对取得良好预后有很大帮助。莫西沙星是一种对革兰氏阳性菌具有广泛活性的新一代氟喹诺酮类药物,已在体外证明其对细胞内细菌储存库有效。通过生存曲线分析以及研究中枢神经系统(CNS)李斯特菌病小鼠模型中血液和器官内细菌生长动力学,在体内比较了莫西沙星和阿莫西林的疗效。我们结合药代动力学和药效学方法,将体内观察到的疗效与血浆和组织中的莫西沙星浓度相关联。与单剂量阿莫西林治疗的动物相比,单剂量莫西沙星治疗的动物死亡显著延迟。我们观察到莫西沙星治疗的动物血液和器官中的细菌迅速清除。血液和大脑中细菌数量的减少与抗生素的血浆和脑内浓度相关。腹腔注射后1小时,莫西沙星在脑中达到峰值,为1.92 +/- 0.32微克/克。这表明莫西沙星能迅速穿过血脑屏障并扩散到脑实质中。此外,在体内实验过程中未筛选出耐药菌株。我们的结果表明,莫西沙星兼具有用的药代动力学特性和快速杀菌活性,可能是治疗中枢神经系统李斯特菌病的一种有价值的替代药物。