Wood M J
Department of Communicable and Tropical Diseases, East Birmingham Hospital, United Kingdom.
Clin Pharmacokinet. 1989;16 Suppl 1:38-45. doi: 10.2165/00003088-198900161-00007.
Enoxacin, in common with other new oral 4-quinolones, has a broad spectrum of antimicrobial activity which includes most pulmonary pathogens (with the exception of Streptococcus pneumoniae, against which its activity is poor); this spectrum has provided the impetus for investigation of its potential in the treatment of respiratory infections. Initial pharmacokinetic studies have demonstrated that the drug has a large volume of distribution and achieves concentrations in the secretions of the respiratory tract that are at least as high as those attained in the serum. These concentrations are sufficient to suggest that enoxacin would be effective treatment for most respiratory infections. Furthermore, the concentration of enoxacin that is achieved within the bronchopulmonary tissues is considerably higher than peak serum concentrations and suggests not only that there is an active transport mechanism, but also that the drug could be expected to eradicate organisms in the lungs such as streptococci that are considered moderately sensitive to the drug in vitro. There are relatively few clinical studies of, and thus limited data on, the efficacy of enoxacin in the treatment of respiratory tract infections. A review of the evidence suggests that enoxacin is as successful as other therapies used in the treatment of acute exacerbations of chronic bronchitis. There have sometimes been failures of eradication of, and occasional superinfections with, pneumococci. Enoxacin is also likely to interact with the metabolism of theophylline and so lead to elevated theophylline plasma concentrations. Hence when these 2 agents are given concurrently, careful monitoring of theophylline concentrations and/or dosage adjustments are recommended.(ABSTRACT TRUNCATED AT 250 WORDS)
依诺沙星与其他新型口服4-喹诺酮类药物一样,具有广泛的抗菌活性,包括大多数肺部病原体(肺炎链球菌除外,其对该药物的活性较差);这种抗菌谱为研究其在治疗呼吸道感染方面的潜力提供了动力。初步的药代动力学研究表明,该药物分布容积大,在呼吸道分泌物中达到的浓度至少与血清中达到的浓度一样高。这些浓度足以表明依诺沙星对大多数呼吸道感染有效。此外,在支气管肺组织中达到的依诺沙星浓度明显高于血清峰值浓度,这不仅表明存在主动转运机制,而且还表明该药物有望根除肺部的病原体,如在体外对该药物中度敏感的链球菌。关于依诺沙星治疗呼吸道感染疗效的临床研究相对较少,因此数据有限。对证据的回顾表明依诺沙星在治疗慢性支气管炎急性加重方面与其他疗法一样成功。有时会出现肺炎球菌清除失败和偶尔的二重感染。依诺沙星也可能与茶碱的代谢相互作用,从而导致茶碱血浆浓度升高。因此,当同时使用这两种药物时,建议仔细监测茶碱浓度和/或调整剂量。(摘要截短至250字)