Abstract
The pharmacokinetics of ceftibuten, a new cephalosporin antibiotic, and its conversion product, ceftibutentrans, were studied in healthy male volunteers following daily oral administration of a 400-mg capsule for 7 days. Mean concentrations of ceftibuten in plasma obtained on day 5 were similar to those obtained on day 7. Analysis of variance indicated that the concentrations in plasma on days 5 and 7 were at steady state. The mean accumulation factor was 1.14 for day 5 and 1.13 for day 7. The half-life (2.4 h) was independent of the duration of drug administration, and the mean maximum concentration of drug in plasma was 18 to 19 micrograms/ml. Urinary excretion was the major elimination route for ceftibuten, by which 57 to 59% of the drug was excreted unchanged over a 24-h period. The amounts of ceftibuten-trans in plasma and urine were low.
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- Barbhaiya R. H., Shukla U. A., Gleason C. R., Shyu W. C., Pittman K. A. Comparison of the effects of food on the pharmacokinetics of cefprozil and cefaclor. Antimicrob Agents Chemother. 1990 Jun;34(6):1210–1213. doi: 10.1128/aac.34.6.1210. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Bauernfeind A. Ceftibuten and bactericidal kinetics. Comparative in vitro activity against Enterobacteriaceae producing extended spectrum beta-lactamases. Diagn Microbiol Infect Dis. 1991 Jan-Feb;14(1):89–92. doi: 10.1016/0732-8893(91)90095-w. [DOI] [PubMed] [Google Scholar]
- Bauernfeind A. Comparative antimicrobial spectrum and activity of ceftibuten against clinical isolates from West Germany. Diagn Microbiol Infect Dis. 1991 Jan-Feb;14(1):63–74. doi: 10.1016/0732-8893(91)90091-s. [DOI] [PubMed] [Google Scholar]
- Blouin R. A., Kneer J., Stoeckel K. Pharmacokinetics of intravenous cefetamet (Ro 15-8074) and oral cefetamet pivoxil (Ro 15-8075) in young and elderly subjects. Antimicrob Agents Chemother. 1989 Mar;33(3):291–296. doi: 10.1128/aac.33.3.291. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Chirurgi V. A., Edelstein H., Oster S. E., Karp R., Cassano K. B., Aiken S., Krumpe P., McCabe R. E. Ceftibuten versus cefaclor for the treatment of bronchitis. J Antimicrob Chemother. 1991 Oct;28(4):577–580. doi: 10.1093/jac/28.4.577. [DOI] [PubMed] [Google Scholar]
- De Abate C. A., Perrotta R. J., Dennington M. L., Ziering R. M. The efficacy and safety of once-daily ceftibuten compared with co-amoxiclav in the treatment of acute bacterial sinusitis. J Chemother. 1992 Dec;4(6):358–363. doi: 10.1080/1120009x.1992.11739192. [DOI] [PubMed] [Google Scholar]
- Deppermann K. M., Lode H., Höffken G., Tschink G., Kalz C., Koeppe P. Influence of ranitidine, pirenzepine, and aluminum magnesium hydroxide on the bioavailability of various antibiotics, including amoxicillin, cephalexin, doxycycline, and amoxicillin-clavulanic acid. Antimicrob Agents Chemother. 1989 Nov;33(11):1901–1907. doi: 10.1128/aac.33.11.1901. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Faix R. G. Parvovirus and neonatal hydrops. Pediatr Infect Dis J. 1993 Jun;12(6):545–545. doi: 10.1097/00006454-199306000-00025. [DOI] [PubMed] [Google Scholar]
- Faulkner R. D., Bohaychuk W., Haynes J. D., Desjardins R. E., Yacobi A., Silber B. M. The pharmacokinetics of cefixime in the fasted and fed state. Eur J Clin Pharmacol. 1988;34(5):525–528. doi: 10.1007/BF01046715. [DOI] [PubMed] [Google Scholar]
- Harding S. M., Williams P. E., Ayrton J. Pharmacology of Cefuroxime as the 1-acetoxyethyl ester in volunteers. Antimicrob Agents Chemother. 1984 Jan;25(1):78–82. doi: 10.1128/aac.25.1.78. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Hill H. R. Intravenous immunoglobulin use in the neonate: role in prophylaxis and therapy of infection. Pediatr Infect Dis J. 1993 Jul;12(7):549–559. [PubMed] [Google Scholar]
- Jones R. N., Barry A. L. Ceftibuten (7432-S, SCH 39720): comparative antimicrobial activity against 4735 clinical isolates, beta-lactamase stability and broth microdilution quality control guidelines. Eur J Clin Microbiol Infect Dis. 1988 Dec;7(6):802–807. doi: 10.1007/BF01975055. [DOI] [PubMed] [Google Scholar]
- Stein G. E., Christensen S., Mummaw N. Treatment of acute uncomplicated urinary tract infection with ceftibuten. Infection. 1991 Mar-Apr;19(2):124–126. doi: 10.1007/BF01645584. [DOI] [PubMed] [Google Scholar]
- Wise R., Andrews J. M., Ashby J. P., Thornber D. Ceftibuten: a new orally absorbed cephalosporin. In vitro activity against strains from the United Kingdom. Diagn Microbiol Infect Dis. 1991 Jan-Feb;14(1):45–52. doi: 10.1016/0732-8893(91)90089-x. [DOI] [PubMed] [Google Scholar]