Abstract
The pharmacokinetics of oral fluoroquinolone antibiotics in normal volunteers have been studied extensively; however, limited patient data exist. Enoxacin steady-state pharmacokinetics and bioavailability were determined following repeated 400-mg intravenous (i.v.) and oral dosing by using compartmental and noncompartmental methods in 10 elderly (mean age, 73.8 years) men with complicated urinary tract infections. Average peak enoxacin concentrations following i.v. and oral dosing were 8.15 and 5.45 mg/liter, respectively. Mean values for major pharmacokinetic parameters (noncompartmental) were similar following i.v. and oral administration, respectively: area under the concentration-time curve from 0 to 12 h, 47.6 and 41.0 mg.h/liter; volume of distribution or volume of distribution/bioavailability, 1.61 and 1.99 liters/kg; total body clearance or total body clearance/bioavailability, 2.58 and 3.01 ml/min per kg; and half-life, 8.2 and 9.1 h. Parameters from analysis of enoxacin plasma concentration data by using a two-compartment pharmacokinetic model also revealed marked similarities between the two administration routes. Enoxacin was highly bioavailable (mean, 86.97%) following oral administration.
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Selected References
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- Ball A. P., Fox C., Ball M. E., Brown I. R., Willis J. V. Pharmacokinetics of oral ciprofloxacin, 100 mg single dose, in volunteers and elderly patients. J Antimicrob Chemother. 1986 May;17(5):629–635. doi: 10.1093/jac/17.5.629. [DOI] [PubMed] [Google Scholar]
- Blaser J., Stone B. B., Groner M. C., Zinner S. H. Comparative study with enoxacin and netilmicin in a pharmacodynamic model to determine importance of ratio of antibiotic peak concentration to MIC for bactericidal activity and emergence of resistance. Antimicrob Agents Chemother. 1987 Jul;31(7):1054–1060. doi: 10.1128/aac.31.7.1054. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Bury R. W., Becker G. J., Kincaid-Smith P. S., Moulds R. F., Whitworth J. A. Elimination of enoxacin in renal disease. Clin Pharmacol Ther. 1987 Apr;41(4):434–438. doi: 10.1038/clpt.1987.53. [DOI] [PubMed] [Google Scholar]
- Cockcroft D. W., Gault M. H. Prediction of creatinine clearance from serum creatinine. Nephron. 1976;16(1):31–41. doi: 10.1159/000180580. [DOI] [PubMed] [Google Scholar]
- Dobbs B. R., Gazeley L. R., Campbell A. J., Edwards I. R. The effect of age on the pharmacokinetics of enoxacin. Eur J Clin Pharmacol. 1987;33(1):101–104. doi: 10.1007/BF00610390. [DOI] [PubMed] [Google Scholar]
- Greenblatt D. J., Sellers E. M., Shader R. I. Drug therapy: drug disposition in old age. N Engl J Med. 1982 May 6;306(18):1081–1088. doi: 10.1056/NEJM198205063061804. [DOI] [PubMed] [Google Scholar]
- Henwood J. M., Monk J. P. Enoxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs. 1988 Jul;36(1):32–66. doi: 10.2165/00003495-198836010-00004. [DOI] [PubMed] [Google Scholar]
- LeBel M., Barbeau G., Bergeron M. G., Roy D., Vallée F. Pharmacokinetics of ciprofloxacin in elderly subjects. Pharmacotherapy. 1986 Mar-Apr;6(2):87–91. doi: 10.1002/j.1875-9114.1986.tb03458.x. [DOI] [PubMed] [Google Scholar]
- Ljungberg B., Nilsson-Ehle I. Pharmacokinetics of antimicrobial agents in the elderly. Rev Infect Dis. 1987 Mar-Apr;9(2):250–264. doi: 10.1093/clinids/9.2.250. [DOI] [PubMed] [Google Scholar]
- Naber K. G., Sörgel F., Gutzler F., Bartosik-Wich B. In vitro activity, pharmacokinetics, clinical safety and therapeutic efficacy of enoxacin in the treatment of patients with complicated urinary tract infections. Infection. 1985 Sep-Oct;13(5):219–224. doi: 10.1007/BF01667215. [DOI] [PubMed] [Google Scholar]
- Neuman M. Clinical pharmacokinetics of the newer antibacterial 4-quinolones. Clin Pharmacokinet. 1988 Feb;14(2):96–121. doi: 10.2165/00003088-198814020-00003. [DOI] [PubMed] [Google Scholar]
- Nix D. E., Schultz R. W., Frost R. W., Sedman A. J., Thomas D. J., Kinkel A. W., Schentag J. J. The effect of renal impairment and haemodialysis on single dose pharmacokinetics of oral enoxacin. J Antimicrob Chemother. 1988 Feb;21 (Suppl B):87–95. doi: 10.1093/jac/21.suppl_b.87. [DOI] [PubMed] [Google Scholar]
- Reeves D. S., Bywater M. J., Holt H. A. The activity of enoxacin against clinical bacterial isolates in comparison with that of five other agents, and factors affecting that activity. J Antimicrob Chemother. 1984 Sep;14 (Suppl 100):7–17. doi: 10.1093/jac/14.suppl_c.7. [DOI] [PubMed] [Google Scholar]
- Smith I. L., Schentag J. J. Noncompartmental determination of the steady-state volume of distribution during multiple dosing. J Pharm Sci. 1984 Feb;73(2):281–282. doi: 10.1002/jps.2600730239. [DOI] [PubMed] [Google Scholar]
- Toothaker R. D. Enoxacin absorption and elimination characteristics. Clin Pharmacokinet. 1989;16 (Suppl 1):52–58. doi: 10.2165/00003088-198900161-00009. [DOI] [PubMed] [Google Scholar]
- Van der Auwera P., Stolear J. C., George B., Dudley M. N. Pharmacokinetics of enoxacin and its oxometabolite following intravenous administration to patients with different degrees of renal impairment. Antimicrob Agents Chemother. 1990 Aug;34(8):1491–1497. doi: 10.1128/aac.34.8.1491. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Wise R., Baker S. L., Misra M., Griggs D. The pharmacokinetics of enoxacin in elderly patients. J Antimicrob Chemother. 1987 Mar;19(3):343–350. doi: 10.1093/jac/19.3.343. [DOI] [PubMed] [Google Scholar]
- Wolf R., Eberl R., Dunky A., Mertz N., Chang T., Goulet J. R., Latts J. The clinical pharmacokinetics and tolerance of enoxacin in healthy volunteers. J Antimicrob Chemother. 1984 Sep;14 (Suppl 100):63–69. doi: 10.1093/jac/14.suppl_c.63. [DOI] [PubMed] [Google Scholar]
