Yokota T
Yokota Chemotherapy Research Association.
Nihon Rinsho. 1997 May;55(5):1155-60.
Hardness of development of drug-resistant bacteria has cross relation with mechanisms of antibacterial activities of antimicrobial agents. When the site of action of certain antibiotic is single enzyme and the enzyme can be converted to tolerant against the antibiotic by change of single amino acid retaining the enzymatic activity, drug-resistant bacteria can emerge easily. On the other hand, if the site of action is complex metabolic reactions, the drug-resistant bacteria would emerge hardly, because multiple mutations are required in this case. So that knowledges of mechanisms of antimicrobial agents are important to prevent the development of drug-resistant bacteria. Antimicrobial agents are classified into several categories, i.e. inhibitors for bacterial cell wall such as beta-lactam drugs, fosfomycin, and vancomycin; inhibitors for protein biosynthesis such as tetracyclibnes, macrolides, aminoglycoside antibiotics; inhibitors for DNA synthesis such as 4-quinolones; inhibitors for RNA synthesis such as rifampicin.
耐药菌产生的难易程度与抗菌药物的抗菌作用机制存在交叉关系。当某种抗生素的作用位点是单一酶,且该酶可通过单个氨基酸的改变而转变为对该抗生素耐受但仍保留酶活性时,耐药菌很容易出现。另一方面,如果作用位点是复杂的代谢反应,那么耐药菌就很难出现,因为在这种情况下需要多个突变。所以了解抗菌药物的作用机制对于预防耐药菌的产生很重要。抗菌药物可分为几类,即细菌细胞壁抑制剂,如β-内酰胺类药物、磷霉素和万古霉素;蛋白质生物合成抑制剂,如四环素类、大环内酯类、氨基糖苷类抗生素;DNA合成抑制剂,如4-喹诺酮类;RNA合成抑制剂,如利福平。