Monk J P, Campoli-Richards D M
Drugs. 1987 Apr;33(4):346-91. doi: 10.2165/00003495-198733040-00003.
Ofloxacin is one of a new generation of fluorinated quinolones structurally related to nalidixic acid. It is an orally administered broad spectrum antibacterial drug active against most Gram-negative bacteria, many Gram-positive bacteria and some anaerobes. Ciprofloxacin is the only other quinolone with superior in vitro antibacterial activity. However, the pharmacokinetic profile of ofloxacin is superior to that of ciprofloxacin, with more rapid absorption and a peak serum concentration several times higher. Moreover, ofloxacin achieves high concentrations in most tissues and body fluids. The results of clinical trials with ofloxacin have confirmed the potential for use in a wide range of infections, which was indicated by its in vitro antibacterial and pharmacokinetic profiles. It has proven effective against a high percentage of infections caused by Gram-negative organisms, slightly less effective against Gram-positive infections, and effective against some anaerobic infections. Clinical efficacy has also been confirmed in a variety of systemic infections as well as in acute and chronic urinary tract infections, and ofloxacin has generally appeared to be at least as effective as alternative orally administered antibacterial drugs. Ofloxacin is well tolerated and, although experience with the drug in clinical practice to date is limited, bacterial resistance does not appear to develop readily. Thus, ofloxacin is an orally active drug which offers a valuable alternative to other broad spectrum antibacterial drugs.
氧氟沙星是与萘啶酸结构相关的新一代氟喹诺酮类药物之一。它是一种口服的广谱抗菌药物，对大多数革兰氏阴性菌、许多革兰氏阳性菌和一些厌氧菌具有活性。环丙沙星是另一种体外抗菌活性更强的喹诺酮类药物。然而，氧氟沙星的药代动力学特征优于环丙沙星，吸收更快，血清峰值浓度高出数倍。此外，氧氟沙星在大多数组织和体液中都能达到高浓度。氧氟沙星的临床试验结果证实了其在广泛感染中的应用潜力，这在其体外抗菌和药代动力学特征中已有体现。它已被证明对革兰氏阴性菌引起的高比例感染有效，对革兰氏阳性菌感染的有效性略低，对一些厌氧菌感染也有效。在各种全身性感染以及急性和慢性尿路感染中，临床疗效也得到了证实，而且氧氟沙星通常似乎至少与其他口服抗菌药物一样有效。氧氟沙星耐受性良好，尽管目前在临床实践中使用该药物的经验有限，但细菌耐药性似乎不易产生。因此，氧氟沙星是一种口服活性药物，为其他广谱抗菌药物提供了有价值的替代品。
