Labia R, Morand A, Tiwari K, Sirot D, Chanal C
Muséum National d'Histoire Naturelle, CNRS, Paris, France.
J Antimicrob Chemother. 1989 Sep;24 Suppl A:219-23. doi: 10.1093/jac/24.suppl_a.219.
The interactions of a meropenem were studied with a set of beta-lactamases including the new TEM- and SHV-related plasmid-mediated enzymes that have extended-spectrum activity against third-generation cephalosporins ('cefotaximases' and 'ceftazidimases'). Meropenem and imipenem were highly resistant to the hydrolytic activity of all the TEM and SHV related beta-lactamases, and to the OXA enzymes, as were the cephamycins: cefoxitin and cefotetan. The two carbapenems were also highly stable to Class C beta-lactamases (chromosomal cephalosporinases) whereas third-generation cephalosporins and cephamycins were slowly hydrolyzed. Both carbapenems demonstrated quite similar affinities for all the enzymes studied. In some instances, and particularly with Class A (TEM- and SHV-derived) enzymes, meropenem inactivated the beta-lactamase activity. Imipenem appeared less reactive in this respect.
研究了美罗培南与一组β-内酰胺酶的相互作用，这些β-内酰胺酶包括新的与TEM和SHV相关的质粒介导酶，它们对第三代头孢菌素具有超广谱活性（“头孢噻肟酶”和“头孢他啶酶”）。美罗培南和亚胺培南对所有与TEM和SHV相关的β-内酰胺酶以及OXA酶的水解活性具有高度抗性，头霉素类药物头孢西丁和头孢替坦也是如此。这两种碳青霉烯类药物对C类β-内酰胺酶（染色体头孢菌素酶）也高度稳定，而第三代头孢菌素和头霉素类药物则被缓慢水解。两种碳青霉烯类药物对所有研究的酶都表现出非常相似的亲和力。在某些情况下，特别是对于A类（源自TEM和SHV）酶，美罗培南可使β-内酰胺酶失活。在这方面，亚胺培南的反应性似乎较低。
