Sabath L D
Rev Infect Dis. 1984 Sep-Oct;6 Suppl 3:S643-56. doi: 10.1093/clinids/6.supplement_3.s643.
The mechanisms involved in the susceptibility and resistance of Pseudomonas aeruginosa to antimicrobial agents are varied. For the beta-lactam agents, susceptibility of the organism is dependent on penetration of the outer membrane, binding to target proteins, absence of significant beta-lactamases, and, possibly, the initiation of cell wall lysis. Susceptibility to aminoglycosides is based on membrane permeation and transport and specific binding to the 30S ribosomal subunit. Antipseudomonal activity of the polymyxins is related to their binding to membrane phospholipids, with subsequent disruption of the membrane; and activity of tetracycline and erythromycin, which is pH-dependent, affects protein synthesis. Resistance to beta-lactam agents is mediated through beta-lactamases, the Id and V enzymes being especially important in P. aeruginosa. Other postulated mechanisms of resistance include the presence of a permeability barrier, insensitivity of target sites, decreased binding, and "trapping." Decreased binding to the S12 protein (often termed the P10 protein in references to streptomycin), decreased active transport, and enzyme-mediated modification are the major mechanisms responsible for resistance to aminoglycosides. The factors involved in resistance to tetracycline and erythromycin remain unclear. The emergence of resistance during a single course of beta-lactam therapy is a special problem with P. aeruginosa and may be due to acquisition of resistance genes, cross-infection, selection or induction of resistance in some variants, or mutation.
铜绿假单胞菌对抗菌药物的易感性和耐药性涉及多种机制。对于β-内酰胺类药物,该菌的易感性取决于外膜的通透性、与靶蛋白的结合、不存在显著的β-内酰胺酶,以及可能的细胞壁裂解的起始。对氨基糖苷类药物的易感性基于膜的渗透和转运以及与30S核糖体亚基的特异性结合。多粘菌素的抗铜绿假单胞菌活性与其与膜磷脂的结合有关,随后导致膜的破坏;而四环素和红霉素的活性(其依赖于pH值)影响蛋白质合成。对β-内酰胺类药物的耐药性是由β-内酰胺酶介导的,Ⅰ型和Ⅴ型酶在铜绿假单胞菌中尤为重要。其他推测的耐药机制包括存在通透性屏障、靶位点不敏感、结合减少和“捕获”。与S12蛋白结合减少(在关于链霉素的参考文献中常称为P10蛋白)、主动转运减少和酶介导的修饰是导致对氨基糖苷类药物耐药的主要机制。与四环素和红霉素耐药相关的因素仍不清楚。在单一疗程的β-内酰胺治疗期间耐药性的出现是铜绿假单胞菌的一个特殊问题,可能是由于获得耐药基因、交叉感染、某些变体中耐药性的选择或诱导,或突变所致。