Liu Y C, Huang W K, Cheng D L
Section of Infectious Diseases, Veterans General Hospital - Kaohsiung, Taiwan/ROC.
Chemotherapy. 1997 Jan-Feb;43(1):21-6. doi: 10.1159/000239530.
Cefpodoxime proxetil is a new orally administered prodrug which is absorbed and de-esterified by the intestinal mucosa to release the third-generation cephalosporin, cefpodoxime, and which is undergoing in vitro and in vivo evaluations. Using the standard agar dilution method, we compared the in vitro activity of this drug with other oral cephalosporins and quinolones against 637 recent clinical isolates from Kaohsiung Veterans General Hospital in Taiwan. Against Escherichia coli and Klebsiella pneumoniae, cefpodoxime showed excellent activity, inhibiting over 90% of these isolates at 1 mg/l. Like other oral drugs of its class, it had little activity against Pseudomonas aeruginosa and Acinetobacter spp. Against Haemophilus influenzae, irrespective of beta-lactamase production, its activity was similar to comparative drugs. Against methicillin-susceptible Staphylococcus aureus, cefpodoxime showed moderate activity, inhibiting 90% of these isolates at 4 mg/l, whereas it was inactive against methicillin-resistant S. aureus. However, all cephalosporins have shown little in vivo activity against methicillin-resistant S. aureus regardless of in vitro results. Cefpodoxime was inactive against Enterococcus spp. Against other streptococci, its activity was similar to other oral cephalosporins and quinolones tested. The results of this in vitro study indicated that oral administration of cefpodoxime should be an ideal agent in the empirical outpatient treatment for community-acquired cutaneous, respiratory and urinary tract infections.
头孢泊肟酯是一种新型口服前体药物,可被肠黏膜吸收并去酯化,从而释放出第三代头孢菌素头孢泊肟,目前正在进行体外和体内评估。我们采用标准琼脂稀释法,比较了该药物与其他口服头孢菌素和喹诺酮类药物对来自台湾高雄荣民总医院的637株近期临床分离菌株的体外活性。对于大肠杆菌和肺炎克雷伯菌,头孢泊肟显示出优异的活性,在1mg/l时可抑制超过90%的这些分离菌株。与同类其他口服药物一样,它对铜绿假单胞菌和不动杆菌属几乎没有活性。对于流感嗜血杆菌,无论其β-内酰胺酶产生情况如何,其活性与对照药物相似。对于甲氧西林敏感金黄色葡萄球菌,头孢泊肟显示出中等活性,在4mg/l时可抑制90%的这些分离菌株,而对甲氧西林耐药金黄色葡萄球菌无活性。然而,无论体外结果如何,所有头孢菌素对甲氧西林耐药金黄色葡萄球菌的体内活性都很低。头孢泊肟对肠球菌属无活性。对于其他链球菌,其活性与所测试的其他口服头孢菌素和喹诺酮类药物相似。这项体外研究的结果表明,口服头孢泊肟应该是社区获得性皮肤、呼吸道和泌尿道感染经验性门诊治疗的理想药物。