Ullmann U
Zentralbl Bakteriol Mikrobiol Hyg A Med Mikrobiol Infekt Parasitol. 1982 Jun;252(2):222-9.
MIC's of beta-lactamase producing strains of P. aeruginosa, E. coli, P. vulgaris, P. rettgeri, E. cloacae, K. pneumoniae, S. marcescens are determined against piperacillin and in the case of S. aureus against amoxycillin and penicillin G. All the strains studied were resistant to these antibiotics. Their MIC's were determined in the combination with different concentrations (2, 5, 10 mg/l) of clavulanic acid and penicillanic acid sulfone respectively. The combination of piperacillin and clavulanic acid acts synergisticly against Klebsiella sp., indolpositive Proteus sp., and E. coli. Penicillanic acid sulfone was less active than clavulanic acid apart from indolpositive Proteus sp. Against S. aureus however both inhibitors showed the same synergistic efficacy. In detail both inhibitors are very active against constitutive penicillinase, they also exhibited a good activity against Type OXA-2, OXA-3 and SHV-1 beta-lactamase; they were less active to Type TEM-1 and OXA-1 enzyme and did not work against Type Ib, TEM-2 and Type IV beta-lactamase. In investigations using the biophotometer it could be demonstrated that the beta-lactamase inhibitor and the penicillin should be given simultaneously in order to obtain an optimal synergistic effect.
测定了产β-内酰胺酶的铜绿假单胞菌、大肠杆菌、普通变形杆菌、雷氏普罗威登斯菌、阴沟肠杆菌、肺炎克雷伯菌、黏质沙雷氏菌对哌拉西林的最低抑菌浓度(MIC),对于金黄色葡萄球菌则测定了其对阿莫西林和青霉素G的最低抑菌浓度。所有研究的菌株均对这些抗生素耐药。分别测定了它们与不同浓度(2、5、10mg/L)的克拉维酸和青霉素烷砜的联合最低抑菌浓度。哌拉西林与克拉维酸的联合对克雷伯菌属、吲哚阳性变形杆菌属和大肠杆菌具有协同作用。除吲哚阳性变形杆菌属外,青霉素烷砜的活性低于克拉维酸。然而,对于金黄色葡萄球菌,两种抑制剂均显示出相同的协同效果。具体而言,两种抑制剂对组成型青霉素酶均非常有效,它们对OXA-2、OXA-3和SHV-1型β-内酰胺酶也表现出良好的活性;它们对TEM-1和OXA-1型酶的活性较低,对Ib型、TEM-2和IV型β-内酰胺酶无效。在使用生物光度计的研究中可以证明,β-内酰胺酶抑制剂和青霉素应同时给药,以获得最佳的协同效果。