Abstract
Amifloxacin pharmacokinetics after a single oral dose in healthy elderly subjects were determined. Five males and five females aged 65 to 79 years and having creatinine clearances of 39.3 to 87.2 ml/h per kg of body weight were given a 200-mg amifloxacin caplet following an overnight fast. Mean (standard deviation) pharmacokinetic parameters for amifloxacin were as follows: maximum observed concentration in plasma, 1.13 (0.48) and 1.95 (0.52) micrograms/ml; half-life, 5.37 (0.96) and 4.47 (0.87) h; total plasma clearance (unadjusted for fraction absorbed), 259 (53) and 199 (55) ml/h per kg; renal clearance, 113 (20) and 86 (26) ml/h per kg; Varea/F (Varea is volume of distribution; F is fraction absorbed), 2.05 (0.75) and 1.28 (0.39) liter/kg; and amifloxacin excreted in the urine, 42.5% (14.5%) and 42.8% (10.6%) for males and females, respectively. There were no statistically significant differences in pharmacokinetic parameters between sexes that could not be attributed to differences in body weight. Except for a modest 23% reduction in renal clearance and the suggestion of reduced bioavailability, mean values of pharmacokinetic parameters for elderly male subjects were similar to those previously determined for younger male volunteers. Therefore, a modification in amifloxacin dosage regimen based solely on age may not be necessary.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Bayer A., Gajewska A., Stephens M., Stark J. M., Pathy J. Pharmacokinetics of ciprofloxacin in the elderly. Respiration. 1987;51(4):292–295. doi: 10.1159/000195216. [DOI] [PubMed] [Google Scholar]
- Brumfitt W., Franklin I., Grady D., Hamilton-Miller J. M., Iliffe A. Changes in the pharmacokinetics of ciprofloxacin and fecal flora during administration of a 7-day course to human volunteers. Antimicrob Agents Chemother. 1984 Nov;26(5):757–761. doi: 10.1128/aac.26.5.757. [DOI] [PMC free article] [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]
- Felmingham D., Wall R. A. The comparative activity of twelve 4-quinolone antimicrobials and sulphadiazine against Neisseria meningitidis. Drugs Exp Clin Res. 1985;11(7):427–429. [PubMed] [Google Scholar]
- Gonzalez M. A., Uribe F., Moisen S. D., Fuster A. P., Selen A., Welling P. G., Painter B. Multiple-dose pharmacokinetics and safety of ciprofloxacin in normal volunteers. Antimicrob Agents Chemother. 1984 Nov;26(5):741–744. doi: 10.1128/aac.26.5.741. [DOI] [PMC free article] [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]
- Neu H. C., Labthavikul P. Antibacterial activity of amifloxacin (WIN 49, 375), a new quinolone agent. Diagn Microbiol Infect Dis. 1985 Nov;3(6):469–478. doi: 10.1016/s0732-8893(85)80003-1. [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]
- Wentland M. P., Bailey D. M., Cornett J. B., Dobson R. A., Powles R. G., Wagner R. B. Novel amino-substituted 3-quinolinecarboxylic acid antibacterial agents: synthesis and structure-activity relationships. J Med Chem. 1984 Sep;27(9):1103–1108. doi: 10.1021/jm00375a003. [DOI] [PubMed] [Google Scholar]