Ishibiki K, Aikawa N
Nihon Geka Gakkai Zasshi. 1984 Sep;85(9):1133-7.
The third generation cephems, Cefotaxime, Ceftizoxime, Cefmenoxime and Latamoxef, have been developed to aim opportunistic Gram negative pathogens and applied for surgical infections since 1980. Although they have excellent antibacterial activities in vitro against Enterobacter spp., indole positive Proteus spp., Pseudomonas spp. and Bacteroides spp., they show lower activities against Gram positive bacteria. Their pharmacokinetic characteristics are longer serum half-life, lower urinary excretion and higher biliary transmission without any metabolic inactivation in human body. Clinical trials of the third generation cephems to surgical infections in Japan revealed the average efficacy rate of 84% which might be better than that of the second generation cephems. It may be a discrepancy between their antibacterial spectrum and clinical results that responses in cases caused by Gram negatives did not exceed those by Gram positives. Clinical application of the third generation cephems should be limited to the surgical infections caused by Gram negatives in immunocompromised host to avoid the emergence of resistant strains.
第三代头孢菌素,如头孢噻肟、头孢唑肟、头孢甲肟和拉氧头孢,是针对机会性革兰氏阴性病原菌研发的,自1980年起应用于外科感染。尽管它们在体外对肠杆菌属、吲哚阳性变形杆菌属、假单胞菌属和拟杆菌属具有优异的抗菌活性,但对革兰氏阳性菌的活性较低。它们的药代动力学特征是血清半衰期较长、尿排泄较低、胆汁排泄较高,且在人体内无任何代谢失活。日本对第三代头孢菌素用于外科感染的临床试验显示,平均有效率为84%,可能优于第二代头孢菌素。革兰氏阴性菌引起的病例反应未超过革兰氏阳性菌引起的病例反应,这可能是它们的抗菌谱与临床结果之间的差异。第三代头孢菌素的临床应用应限于免疫功能低下宿主中由革兰氏阴性菌引起的外科感染,以避免耐药菌株的出现。