Campoli-Richards D M, Monk J P, Price A, Benfield P, Todd P A, Ward A
ADIS Drug Information Services, Auckland.
Drugs. 1988 Apr;35(4):373-447. doi: 10.2165/00003495-198835040-00003.
Ciprofloxacin is one of a new generation of fluorinated quinolones structurally related to nalidixic acid. The primary mechanism of action of ciprofloxacin is inhibition of bacterial DNA gyrase. It is a broad spectrum antibacterial drug to which most Gram-negative bacteria are highly susceptible in vitro and many Gram-positive bacteria are susceptible or moderately susceptible. Unlike most broad spectrum antibacterial drugs, ciprofloxacin is effective after oral or intravenous administration. Ciprofloxacin has been most extensively studied following oral administration. It attains concentrations in most tissues and body fluids which are at least equivalent to the minimum inhibitory concentration designated as the breakpoint for bacterial susceptibility in vitro. The results of clinical trials with orally and intravenously administered ciprofloxacin have confirmed the potential for its use in a wide range of infections, which was suggested by its in vitro antibacterial and pharmacokinetic profiles. It has proven an effective treatment for many types of systemic infections as well as for both acute and chronic infections of the urinary tract. Ciprofloxacin generally appeared to be at least as effective as alternative orally administered antibacterial drugs in the indications in which they were compared, and in some indications, to parenterally administered antibacterial therapy. However, further studies are needed to fully clarify the comparative efficacy of ciprofloxacin and standard antibacterial therapies. Bacterial resistance to ciprofloxacin develops infrequently, both in vitro and clinically, except in the setting of pseudomonal respiratory tract infections in cystic fibrosis patients. The drug is also well tolerated. Thus, as an orally active, broad spectrum and potent antibacterial drug, ciprofloxacin offers a valuable alternative to broad spectrum parenterally administered antibacterial drugs for use in a wide range of clinical infections, including difficult infections due to multiresistant pathogens.
环丙沙星是与萘啶酸结构相关的新一代氟喹诺酮类药物之一。环丙沙星的主要作用机制是抑制细菌DNA回旋酶。它是一种广谱抗菌药物，大多数革兰氏阴性菌在体外对其高度敏感，许多革兰氏阳性菌对其敏感或中度敏感。与大多数广谱抗菌药物不同，环丙沙星口服或静脉给药后均有效。环丙沙星口服给药后得到了最广泛的研究。它在大多数组织和体液中达到的浓度至少相当于体外细菌敏感性断点指定的最低抑菌浓度。口服和静脉注射环丙沙星的临床试验结果证实了其在广泛感染中的应用潜力，这一点从其体外抗菌和药代动力学特征中可以看出。它已被证明对多种类型的全身感染以及泌尿系统的急性和慢性感染均有效。在比较的适应症中，环丙沙星通常至少与其他口服抗菌药物一样有效，在某些适应症中，与胃肠外给药的抗菌治疗效果相当。然而，需要进一步研究以充分阐明环丙沙星与标准抗菌治疗的比较疗效。除了囊性纤维化患者的假单胞菌呼吸道感染外，细菌对环丙沙星的耐药性在体外和临床上都很少出现。该药物耐受性也良好。因此，作为一种口服活性、广谱且强效的抗菌药物，环丙沙星为胃肠外给药的广谱抗菌药物提供了一种有价值的替代品，可用于广泛的临床感染，包括由多重耐药病原体引起的难治性感染。
