Bauernfeind A, Jungwirth R, Schweighart S, Theopold M
Max von Pettenkofer-Institut, München, Germany.
Infection. 1990;18 Suppl 3:S155-67. doi: 10.1007/BF01644637.
Oral cephalosporins (cefixime, cefdinir, cefetamet, ceftibuten, cefpodoxime, loracarbef, cefprozil, cefuroxime, cefaclor, cefadroxil and BAY 3522) were compared by their antibacterial profile including stability against new beta-lactamases. Both activity and antibacterial spectrum of compounds structurally related to third generation parenteral cephalosporins (of the oximino class) were superior to established compounds. Activity against staphylococci was found to be highest for cefdinir, cefprozil and BAY 3522. Cefetamet, ceftibuten and cefixime demonstrate no clinically meaningful antistaphylococcal activity while the other compounds investigated demonstrate intermediate activity. The antibacterial spectrum was broadest for cefdinir and cefpodoxime. New oral cephalosporins are equally inactive as established compounds against Enterobacter spp., Morganella, Listeria, Pseudomonas and Acinetobacter spp., methicillin-resistant staphylococci, Enterococcus spp., penicillin-resistant pneumococci and anaerobes. New extended broad-spectrum betalactamases (TEM-3, TEM-5, TEM-6, TEM-7, SHV-2, SHV-3, SHV-4, SHV-5, CMY-1, CMY-2, and CTX-M) are active against the majority of oral cephalosporins. Ceftibuten, cefetamet, cefixime and cefdinir were stable against some of these enzymes even to a higher extent than parenteral cephalosporins. New oral cephalosporins should improve the therapeutic perspectives of oral cephalosporins due to their higher activity against pathogens marginally susceptible to established compounds (higher multiplicity of maximum plasma concentrations over MICs of the pathogens) and furthermore by including in their spectrum organisms resistant to established absorbable cephalosporins (e.g. Proteus spp., Providencia spp., Citrobacter spp., and Serratia spp.).
对口服头孢菌素（头孢克肟、头孢地尼、头孢他美、头孢布烯、头孢泊肟、氯碳头孢、头孢丙烯、头孢呋辛、头孢克洛、头孢羟氨苄和BAY 3522）的抗菌谱进行了比较，包括对新型β-内酰胺酶的稳定性。与第三代肠外头孢菌素（肟类）结构相关的化合物的活性和抗菌谱均优于已有的化合物。发现头孢地尼、头孢丙烯和BAY 3522对葡萄球菌的活性最高。头孢他美、头孢布烯和头孢克肟无临床意义的抗葡萄球菌活性，而所研究的其他化合物表现出中等活性。头孢地尼和头孢泊肟的抗菌谱最广。新型口服头孢菌素与已有的化合物一样，对肠杆菌属、摩根菌属、李斯特菌属、假单胞菌属和不动杆菌属、耐甲氧西林葡萄球菌、肠球菌属、耐青霉素肺炎球菌和厌氧菌均无活性。新型超广谱β-内酰胺酶（TEM-3、TEM-5、TEM-6、TEM-7、SHV-2、SHV-3、SHV-4、SHV-5、CMY-1、CMY-2和CTX-M）对大多数口服头孢菌素具有活性。头孢布烯、头孢他美、头孢克肟和头孢地尼对其中一些酶稳定，甚至比肠外头孢菌素更稳定。新型口服头孢菌素应能改善口服头孢菌素的治疗前景，因为它们对仅对已有化合物轻度敏感的病原体具有更高的活性（病原体的最大血浆浓度与最低抑菌浓度的倍数更高），而且其抗菌谱还包括对已有可吸收头孢菌素耐药的微生物（如变形杆菌属、普罗威登斯菌属、柠檬酸杆菌属和沙雷菌属）。
