Labia R, Morand A, Verchere-Beaur C, Amrani R, Beklahia C
Presse Med. 1986 Dec 20;15(46):2303-8.
Like all penicillins, piperacillin exhibits some susceptibility to beta-lactamases of the penicillinase type, including those produced by Staphylococcus aureus and the TEM, OXA and CARB enzymes isolated from Gram-negative bacilli. Piperacillin is very slightly hydrolyzed by cephalosporinases, which makes it similar to 3rd generation cephalosporins. When tested with Enterobacter cloacae GN 5797 and Pseudomonas aeruginosa NTC 8303, two strains which produce inducible cephalosporinases, piperacillin had moderate inductive activity compared to cefoxitin, a potent inducer. Induction was very low with Enterobacter, but the drug was slightly more sensitive to Pseudomonas. Inhibition of this type of beta-lactamase synthesis was very strong when piperacillin was combined with amikacin and weaker when it was combined with pefloxacin. The piperacillin-amikacin combination prevented the development of piperacillin-resistant mutants of Enterobacter and Pseudomonas and, probably, of all Gram-negative bacilli. In our tests, the piperacillin-pefloxacin combination was of interest only against Enterobacter, and probably against all enterobacteria, since Pseudomonas mutants that resist pefloxacin are fairly easily obtained in vitro.
与所有青霉素一样，哌拉西林对青霉素酶类型的β-内酰胺酶表现出一定的敏感性，包括金黄色葡萄球菌产生的酶以及从革兰氏阴性杆菌中分离出的TEM、OXA和CARB酶。哌拉西林被头孢菌素酶水解的程度非常轻微，这使其与第三代头孢菌素相似。在用阴沟肠杆菌GN 5797和铜绿假单胞菌NTC 8303这两种可产生诱导型头孢菌素酶的菌株进行测试时，与强效诱导剂头孢西丁相比，哌拉西林具有中等诱导活性。在阴沟肠杆菌中诱导作用非常低，但该药物对铜绿假单胞菌的敏感性略高。当哌拉西林与阿米卡星联合使用时，对这种类型的β-内酰胺酶合成的抑制作用非常强，而与培氟沙星联合使用时则较弱。哌拉西林-阿米卡星组合可防止阴沟肠杆菌和铜绿假单胞菌以及可能所有革兰氏阴性杆菌的哌拉西林耐药突变体的产生。在我们的测试中，哌拉西林-培氟沙星组合仅对阴沟肠杆菌有作用，可能对所有肠杆菌都有作用，因为在体外相当容易获得对培氟沙星耐药的铜绿假单胞菌突变体。
