Dornbusch K, Frolander F, Cacciapuoti A F, Naples L, Hare R S, Miller G H
J Antimicrob Chemother. 1985 Jun;15 Suppl C:85-97. doi: 10.1093/jac/15.suppl_c.85.
The activity of Sch 34343 against 13 strains producing large amounts of characterized beta-lactamases was compared with that of imipenem, latamoxef (moxalactam), aztreonam and other third-generation cephalosporins. Sch 34343, like imipenem, was active against all strains, including many resistant to all other beta-lactams. MICs of Sch 34343 determined for 16 different inocula were rarely increased even at very high inocula. Sch 34343 was rapidly bactericidal against Escherichia coli TEM-2, Enterobacter agglomerans (with an induced beta-lactamase) and two strains of Bacteroides fragilis with highly active cephalosporinases. Like cefoxitin, Sch 34343 was only slowly inactivated by concentrated crude penicillinases which inactivated cefotaxime within 1 h. Sch 34343 was even more stable to cephalosporinases than was cefoxitin. Stability of the antibiotics to the different beta-lactamases was also determined by pre-incubating them with dilutions of the beta-lactamases before determination of MICs against E. coli 25922. Very large amounts of all enzymes were required to increase the MICs significantly for Sch 34343 and imipenem. These results indicate the good stability of Sch 34343 to beta-lactamases.
将Sch 34343对13株产生大量已鉴定β-内酰胺酶菌株的活性与亚胺培南、拉氧头孢(羟羧氧酰胺菌素)、氨曲南及其他第三代头孢菌素进行了比较。Sch 34343与亚胺培南一样,对所有菌株均有活性,包括许多对所有其他β-内酰胺类耐药的菌株。针对16种不同接种量测定的Sch 34343的最低抑菌浓度(MIC),即使在接种量非常高时也很少增加。Sch 34343对大肠杆菌TEM-2、聚团肠杆菌(带有诱导型β-内酰胺酶)以及两株具有高活性头孢菌素酶的脆弱拟杆菌具有快速杀菌作用。与头孢西丁一样,Sch 34343仅被浓缩的粗制青霉素酶缓慢灭活,而这种酶可在1小时内使头孢噻肟失活。Sch 34343对头孢菌素酶的稳定性甚至比头孢西丁更高。在针对大肠杆菌25922测定MIC之前,通过将抗生素与β-内酰胺酶的稀释液预孵育,也确定了抗生素对不同β-内酰胺酶的稳定性。对于Sch 34343和亚胺培南,需要非常大量的所有酶才能显著提高MIC。这些结果表明Sch 34343对β-内酰胺酶具有良好的稳定性。