Labia R, Morand A
National Museum of Natural History, URA 401 CNRS, Paris, France.
Drugs Exp Clin Res. 1994;20(2):43-8.
The interactions of cefdinir, a new orally-active third-generation cephalosporin, with cell-free beta-lactamase preparations were studied in comparison with some other beta-lactams. Cefdinir was very resistant to narrow-spectrum Ambler's class A beta-lactamases, as it was for other oximino beta-lactams: cefotaxime, ceftazidime, cefixime and cefuroxime. Cefaclor showed a low but significant hydrolysis by these beta-lactamases. These class-A enzymes include the widespread plasmid mediated TEM-1, TEM-2, SHV-1 and also the enzymes of Gram-positive penicillinases, such as that produced by S. aureus. The hydrolysis of cefdinir was hardly detectable by the Ambler's class C beta-lactamases (cephalosporinases) produced by E. coli, E. cloacae and M. morganii. A similar conclusion is shown for cefotaxime, ceftazidime, cefixime and cefuroxime: for these beta-lactamases, the hydrolysis of cefaclor was high. The P. vulgaris cephalosporinase differs from the previous cephalosporinases in that it hydrolyses cefotaxime, cefuroxime and cefaclor efficiently. However, the hydrolysis of cefdinir remains too low to be detected. Cefdinir, as other third-generation cephalosporins, showed some hydrolysis by the novel extended-spectrum beta-lactamases (ESBL): SHV-2, TEM-3, TEM-5, MEN-1 and other ESBL.
研究了新型口服活性第三代头孢菌素头孢地尼与无细胞β-内酰胺酶制剂的相互作用,并与其他一些β-内酰胺类药物进行了比较。头孢地尼对窄谱安布勒A类β-内酰胺酶具有很强的抗性,其他肟基β-内酰胺类药物如头孢噻肟、头孢他啶、头孢克肟和头孢呋辛也是如此。头孢克洛被这些β-内酰胺酶水解程度较低但具有显著性。这些A类酶包括广泛存在的质粒介导的TEM-1、TEM-2、SHV-1,以及革兰氏阳性青霉素酶,如金黄色葡萄球菌产生的酶。大肠杆菌、阴沟肠杆菌和摩根氏摩根菌产生的安布勒C类β-内酰胺酶(头孢菌素酶)几乎检测不到头孢地尼的水解。头孢噻肟、头孢他啶、头孢克肟和头孢呋辛也有类似结论:对于这些β-内酰胺酶,头孢克洛的水解程度较高。普通变形杆菌头孢菌素酶与之前的头孢菌素酶不同,它能有效水解头孢噻肟、头孢呋辛和头孢克洛。然而,头孢地尼的水解程度仍然很低,无法检测到。与其他第三代头孢菌素一样,头孢地尼被新型超广谱β-内酰胺酶(ESBL)如SHV-2、TEM-3、TEM-5、MEN-1和其他ESBL水解。