Tissue Penetration and Clinical Efficacy of Enoxacin in Respiratory Tract Infections

Abstract

Enoxacin. in common with other new oraI4-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 prOl'ided the impetus for investigation of its potential in the treatment of respiratory infections.Initial pharmacokinetic studies have demonstrated that the drug has a large )'olume 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 bronchopulmonar.l' tissues is considerably higher than peak serum concentrations and suggests not onl.\' 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 moderatel.\' sensitil'e to the drug in vitro.There are relatively few clinical studies of, and thus limited data on. the ~fJicac.\' of enoxacin in the treatment of respiratory tract infections. A review of the e)'idence 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 superinfect ions with. pneumococci. Enoxacin is also Iikel.\' to interact with the metabolism of theophylline and so lead to elevated theoph.\'lIine plasma concentrations. Hence when these 2 agents are given concurrent/.v. car~rul monitoring of theoph.\'lIine concentrations and/or dosage adjustments are recommended. In more chronic infections. particular/.v those caused by Pseudomonas aeruginosa, enoxacin seems to be ~ffectil'e. but further comparative studies with more conventional intravenous treatments are required.

Distribution kinetics of enoxacin and its metabolite oxoenoxacin in excretory fluids of healthy volunteers

“…Enoxacin [1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid] is a naphthyridine analog of the quinolone antibacterial agents and exhibits high antibacterial activity against a broad spectrum of gram-negative and moderate activity against gram-positive bacteria (31,45). Its pharmacokinetics in healthy volunteers was studied by several investigators (7,39,43).…”

“…The apparent volume of distribution of enoxacin, like that of other gyrase inhibitors, exceeds the body volume by two-to threefold, suggesting extensive localization at intracellular sites. It has been shown to achieve considerable concentrations in various tissues of patients (1,27,45). The main metabolite of enoxacin is 3Ј-oxoenoxacin (Fig.…”

New Improved Quinlone Derivatives Against Infection

“…Generally, the 7-piperazinyl enoxacin have better Gram-negative than Gram-positive antimicrobial potency (Chin & Neu, 1983, Paton & Reeves, 1988, Wood, 1989. Studies revealed that the mode of action of quinolones involves inhibition of essential type II bacterial topoisomerases such as DNA gyrase and topoisomerase IV (Sissi & Palumbo, 2003).…”

Synthesis and biological evaluations of enoxacin carboxamide derivatives

“…Generally, the 7-piperazinyl quinolones which includes enoxacin have better Gramnegative than Gram-positive antimicrobial potency (Wood, 1989;Paton and Reeves, 1988;Chin and Neu, 1983). Studies revealed that the mode of action of quinolones involves inhibition of essential type II bacterial topoisomerases such as DNA gyrase and topoisomerase IV (Sissi and Palumbo, 2003;Anderson and Osheroff, 2001).…”