Labia R
Sem Hop. 1983 Jun 30;59(26):1959-62.
At present, Moxalactam is the beta-lactam antibiotic which shows the greatest resistance to beta-lactamases. Moxalactam has little, if any, interactions with penicillinases, as is also the case of cefoxitin, cefuroxime and cefotaxime. Resistance of Moxalactam to cephalosporinases, however, appears to be related to the unique property of inactivating them. This implies: a specific process which involves the active site of the enzymes; a progressive, or time-dependent, process, which progressively abolishes beta-lactamase activity. This process was observed with most of the tested cephalosporinases. Thus, Moxalactam is the first beta-lactam antibiotic which inactivates beta-lactamases. This is probably why Moxalactam is so resistant to the action of beta-lactamases.
目前,头孢氧哌唑是对β-内酰胺酶表现出最大抗性的β-内酰胺抗生素。头孢氧哌唑与青霉素酶几乎没有相互作用(即便有也很少),头孢西丁、头孢呋辛和头孢噻肟也是如此。然而,头孢氧哌唑对头孢菌素酶的抗性似乎与其使这些酶失活的独特特性有关。这意味着:一个涉及酶活性位点的特定过程;一个渐进的或时间依赖性的过程,该过程会逐渐消除β-内酰胺酶的活性。在大多数测试的头孢菌素酶中都观察到了这个过程。因此,头孢氧哌唑是第一种能使β-内酰胺酶失活的β-内酰胺抗生素。这可能就是头孢氧哌唑对β-内酰胺酶的作用如此具有抗性的原因。