Rouse Mark S, Hein Melanie M, Anguita-Alonso Paloma, Steckelberg James M, Patel Robin
Division of Infectious Diseases, Department of Internal Medicine, Mayo Clinic College of Medicine, Rochester, MN 55905, USA.
Diagn Microbiol Infect Dis. 2006 Aug;55(4):333-6. doi: 10.1016/j.diagmicrobio.2006.01.029. Epub 2006 May 2.
Ceftobiprole (BAL9141) is an investigational cephalosporin active against methicillin- and vancomycin-resistant staphylococci administered as a water-soluble prodrug, ceftobiprole medocaril (BAL5788). Using an immunocompetent murine pneumonia model of Haemophilus influenzae, Enterobacter cloacae, or extended-spectrum beta-lactamase (ESBL) nonproducing or producing Klebsiella pneumoniae pneumonia, we compared results of treatment with ceftobiprole medocaril (71 mg/kg, sc, qid), ceftriaxone (50 mg/kg, im, bid), or cefepime (50 mg/kg, ip, q.i.d.). Results were expressed as median and 25th to 75th percentile log10 colony forming units per gram of lung tissue. Ceftobiprole, ceftriaxone, and cefepime were each more active than was no treatment and were equally active for treatment of experimental H. influenzae, E. cloacae, or ESBL-nonproducing K. pneumoniae pneumonia. For ESBL-producing K. pneumoniae, no differences were detected between no treatment and treatment with ceftobiprole, ceftriaxone, or cefepime. Ceftobiprole is active against H. influenzae, E. cloacae, and ESBL-nonproducing K. pneumoniae in an immunocompetent experimental murine pneumonia model.
头孢比普（BAL9141）是一种处于研究阶段的头孢菌素，对耐甲氧西林和耐万古霉素葡萄球菌具有活性，以水溶性前药头孢比普甲磺酸盐（BAL5788）的形式给药。我们使用了具有免疫活性的小鼠肺炎模型，该模型感染了流感嗜血杆菌、阴沟肠杆菌，或不产超广谱β-内酰胺酶（ESBL）或产ESBL的肺炎克雷伯菌，比较了头孢比普甲磺酸盐（71mg/kg，皮下注射，每日4次）、头孢曲松（50mg/kg，肌肉注射，每日2次）或头孢吡肟（50mg/kg，腹腔注射，每日4次）的治疗结果。结果以每克肺组织的菌落形成单位的中位数和第25至75百分位数的对数表示。头孢比普、头孢曲松和头孢吡肟各自的活性均高于未治疗组，并且在治疗实验性流感嗜血杆菌、阴沟肠杆菌或不产ESBL的肺炎克雷伯菌肺炎方面活性相当。对于产ESBL的肺炎克雷伯菌，未治疗组与头孢比普、头孢曲松或头孢吡肟治疗组之间未检测到差异。在具有免疫活性的实验性小鼠肺炎模型中，头孢比普对流感嗜血杆菌、阴沟肠杆菌和不产ESBL的肺炎克雷伯菌具有活性。
