Kabins S A, Nathan C
Antimicrob Agents Chemother. 1978 Sep;14(3):391-7. doi: 10.1128/AAC.14.3.391.
Eighty-seven isolates of Pseudomonas, Enterobacteriaceae, and Staphylococcus, chosen because of their resistance to other aminoglycosides, were tested for susceptibility to 5-episisomicin. Tests were performed in Mueller-Hinton agar and also, with 38 of these isolates, in Mueller-Hinton broth. Of Enterobacteriaceae, 85 and 95.5% were inhibited by 5 and 10 mug of 5-episisomicin per ml, respectively. Amikacin inhibited 74 and 91% of the strains at 10 and 20 mug/ml, respectively. Fifty-four percent of P. aeruginosa were inhibited by 5-episisomicin and amikacin. Eighty-three percent of S. aureus were inhibited by netilmicin and amikacin, whereas only 50% were inhibited by 5-episisomicin. Isolates resistant to 5-episisomicin were most often resistant to the other aminoglycosides and occurred in gram-negative bacilli that did not carry aminoglycoside-modifying enzymes. Five of 23 isolates that carried a 6'-N-acetyltransferase (AAC-6') and one of two that carried an aminoglycoside 3-acetyltransferase were resistant to and acetylate 5-episisomicin. Strains carrying other aminoglycoside-modifying enzymes were inhibited by 5-episisomicin. Thus, 5-episisomicin is a promising aminoglycoside not attacked by most aminoglycoside-modifying enzymes. Resistance will probably most often be based upon nonenzymatic mechanisms which will also affect other aminoglycosides.
选取了87株假单胞菌、肠杆菌科细菌和葡萄球菌，因其对其他氨基糖苷类药物耐药，对它们进行了5-表异帕米星敏感性测试。测试在穆勒-欣顿琼脂中进行，并且对其中38株菌株也在穆勒-欣顿肉汤中进行了测试。在肠杆菌科细菌中，每毫升5微克和10微克的5-表异帕米星分别抑制了85%和95.5%的菌株。阿米卡星在每毫升10微克和20微克时分别抑制了74%和91%的菌株。54%的铜绿假单胞菌被5-表异帕米星和阿米卡星抑制。83%的金黄色葡萄球菌被奈替米星和阿米卡星抑制，而只有50%被5-表异帕米星抑制。对5-表异帕米星耐药的菌株最常对其他氨基糖苷类药物耐药，并且出现在不携带氨基糖苷类修饰酶的革兰氏阴性杆菌中。23株携带6'-N-乙酰转移酶（AAC-6'）的菌株中有5株以及2株携带氨基糖苷3-乙酰转移酶的菌株中有1株对5-表异帕米星耐药并使其乙酰化。携带其他氨基糖苷类修饰酶的菌株被5-表异帕米星抑制。因此，5-表异帕米星是一种有前景的氨基糖苷类药物，大多数氨基糖苷类修饰酶不会作用于它。耐药性可能最常基于非酶促机制，这也会影响其他氨基糖苷类药物。
