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喹诺酮类是近年来,临床应用较广泛的一种新型广谱抗菌剂。该类药是在萘啶酸基础结构上合成的第二代喹酮类衍生物。由于在喹诺酮母环6位上引进了氟原子,因此不仅对革兰氏阴性菌有较强的抗菌作用,而且对革兰氏阳性菌也有较强的抗菌作用。主要抗菌机理是抑制细菌DNA旋转酶所催化的ATP依赖超螺旋作用,抑制超螺旋化DNA的松弛作用及促双链DNA的破裂作用。具有抗菌谱广,杀菌力强,不易产生耐药性和交叉耐药及副作用少等优点。自八十年代初问世以来,其中氟哌酸(NFX),氟嗪酸(OFX),氟啶酸(ENX),及环丙氟哌酸(CPF)等抗菌剂已被日、美、联邦德国广泛用于临床。本文就喹诺酮类抗生素临床应用概况作一简述。
Quinolones are new broad-spectrum antibacterial agents widely used clinically in recent years. This class of drugs is based on nalidixic acid synthesis of the second generation of quinolone derivatives. Due to the introduction of fluorine atoms at the 6-position of quinolone ring, it not only has strong antibacterial activity against Gram-negative bacteria but also has strong antibacterial activity against Gram-positive bacteria. The main antibacterial mechanism is inhibition of bacterial DNA gyrase catalyzed ATP-dependent supercoiling, inhibition of supercoiled DNA relaxation and double-stranded DNA rupture. With broad antibacterial spectrum, strong bactericidal, not easy to produce resistance and cross-resistance and fewer side effects. Since the advent of the early 1980s, antibacterial agents such as NFX, OFX, ENX, and ciprofloxacin (CPF) have been widely used in Japan, the United States, the Federal Republic of Germany Widely used in clinical. This article gives a brief overview of the clinical application of quinolone antibiotics.