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氟喹诺酮(FQNs)类药物为广谱、强效抗菌剂,对包括金黄色葡萄球菌在内革兰氏阳性菌和包括铜绿假单胞菌在内的革兰氏阴性菌显示良好的活性,因而在临床上被广泛用于感染性疾病的治疗。然而近年来随着FQNs类药物在临床上的广泛使用,细菌对此类药物的耐药性成蔓延趋势,耐药的细菌种类不断增多,耐药的程度也趋加重,耐药菌株的感染治疗成为一个全球性的问题。故有必要对PQNs类药物耐药机制有所了解,以便采取相应对策防止耐药性的蔓延。 1 FQNs类药物的作用机制 FQNs药物的作用机制是干扰细菌细胞的DNA复制,其作用的靶位是拓扑异构酶,这种酶分为两类:第一类是拓扑异构酶Ⅰ和Ⅱ;第二类是拓扑异构酶Ⅱ和Ⅳ,拓扑异构酶Ⅱ又称为DNA促旋酶。FQNs类主要作用于DNA促旋酶和拓扑异
FQNs are broad-spectrum, potent antimicrobial agents that show good activity against Gram-negative bacteria including Staphylococcus aureus and gram-negative bacteria including Pseudomonas aeruginosa In clinical practice is widely used in the treatment of infectious diseases. However, with the widespread use of FQNs in clinical practice, the resistance of bacteria to such drugs is becoming more and more widespread. The number of resistant bacteria is increasing and the degree of resistance is also aggravating. The infection of resistant strains Become a global issue. Therefore, it is necessary to understand the mechanism of drug resistance of PQNs in order to take corresponding measures to prevent the spread of drug resistance. 1 Mechanism of FQNs Drugs The mechanism of action of FQNs drugs is to interfere with the DNA replication of bacterial cells. The targets of the FQNs drugs are topoisomerases. The enzymes are classified into two types: the first is topoisomerase I and II ; The second is topoisomerase II and IV, and topoisomerase II is also known as DNA gyrase. FQNs mainly act on DNA gyrase and topology