Skip to main content
Antimicrobial Agents and Chemotherapy logoLink to Antimicrobial Agents and Chemotherapy
. 1991 Dec;35(12):2521–2525. doi: 10.1128/aac.35.12.2521

Steady-state pharmacokinetics of ciprofloxacin in plasma from patients with nosocomial pneumonia: penetration of the bronchial mucosa.

D Fabre 1, F Bressolle 1, R Gomeni 1, C Arich 1, F Lemesle 1, H Beziau 1, M Galtier 1
PMCID: PMC245424  PMID: 1810184

Abstract

A 30-min intravenous (i.v.) infusion of 200 mg of ciprofloxacin was administered twice daily to 12 patients with nosocomial pneumonia scheduled to undergo diagnostic fiberoptic bronchoscopy. The pharmacokinetics of ciprofloxacin were examined at the presumed steady state after 5 days of treatment. Eleven successive plasma samples were collected in the interval from 0 to 12 h after administration, and bronchial mucosa samples were taken 2 h after administration. Concentrations of drug in all samples were assayed by high-performance liquid chromatography with fluorimetric detection. The results showed that the kinetics in plasma did not differ from those determined previously in healthy volunteers. The mean concentrations in plasma peaked at 4.94 +/- 2.90 mg/liter at the end of infusion. The terminal half-life was 4.95 +/- 2.81 h, and the mean residence time 6.13 +/- 3.17 h. A large volume of distribution was calculated: 2.59 +/- 1.43 liters/kg. Mean total body clearance was 23.3 +/- 10.1 liters/h. The concentrations in bronchial mucosa reached 21.6 +/- 5.63 micrograms/g 2 h after drug intake. The tissue-versus-plasma concentration ratios ranged from 10.1 to 26.3 (mean value, 16.9 +/- 5.43). After 6 to 12 days of i.v. treatment, four patients were switched to oral ciprofloxacin. We propose a model for the simultaneous fit of the concentration-time curves obtained after i.v. infusion and oral dosing. The concentrations in tissue observed in this study were in excess of the MICs for bacteria considered to be susceptible to ciprofloxacin.

Full text

PDF
2521

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Bauernfeind A., Petermüller C. In vitro activity of ciprofloxacin, norfloxacin and nalidixic acid. Eur J Clin Microbiol. 1983 Apr;2(2):111–115. doi: 10.1007/BF02001575. [DOI] [PubMed] [Google Scholar]
  2. Bell R. C., Coalson J. J., Smith J. D., Johanson W. G., Jr Multiple organ system failure and infection in adult respiratory distress syndrome. Ann Intern Med. 1983 Sep;99(3):293–298. doi: 10.7326/0003-4819-99-3-293. [DOI] [PubMed] [Google Scholar]
  3. Brittain D. C., Scully B. E., McElrath M. J., Steinman R., Labthavikul P., Neu H. C. The pharmacokinetics and serum and urine bactericidal activity of ciprofloxacin. J Clin Pharmacol. 1985 Mar;25(2):82–88. doi: 10.1002/j.1552-4604.1985.tb02806.x. [DOI] [PubMed] [Google Scholar]
  4. 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]
  5. Campoli-Richards D. M., Monk J. P., Price A., Benfield P., Todd P. A., Ward A. Ciprofloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs. 1988 Apr;35(4):373–447. doi: 10.2165/00003495-198835040-00003. [DOI] [PubMed] [Google Scholar]
  6. Craven D. E., Kunches L. M., Kilinsky V., Lichtenberg D. A., Make B. J., McCabe W. R. Risk factors for pneumonia and fatality in patients receiving continuous mechanical ventilation. Am Rev Respir Dis. 1986 May;133(5):792–796. [PubMed] [Google Scholar]
  7. Crump B., Wise R., Dent J. Pharmacokinetics and tissue penetration of ciprofloxacin. Antimicrob Agents Chemother. 1983 Nov;24(5):784–786. doi: 10.1128/aac.24.5.784. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Dalhoff A., Eickenberg H. U. Tissue distribution of ciprofloxacin following oral and intravenous administration. Infection. 1985 Mar-Apr;13(2):78–81. doi: 10.1007/BF01660419. [DOI] [PubMed] [Google Scholar]
  9. Davies B. I., Maesen F. P., Baur C. Ciprofloxacin in the treatment of acute exacerbations of chronic bronchitis. Eur J Clin Microbiol. 1986 Apr;5(2):226–231. doi: 10.1007/BF02013995. [DOI] [PubMed] [Google Scholar]
  10. Drusano G. L., Standiford H. C., Plaisance K., Forrest A., Leslie J., Caldwell J. Absolute oral bioavailability of ciprofloxacin. Antimicrob Agents Chemother. 1986 Sep;30(3):444–446. doi: 10.1128/aac.30.3.444. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Fass R. J. In vitro activity of ciprofloxacin (Bay o 9867). Antimicrob Agents Chemother. 1983 Oct;24(4):568–574. doi: 10.1128/aac.24.4.568. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Forst H., Ruckdeschel G., Unertl K., Dieterich H. J., Ehret W., Sunder-Plassmann L. Lung tissue concentrations of ciprofloxacin following intravenous administration in patients. Arzneimittelforschung. 1989 May;39(5):618–619. [PubMed] [Google Scholar]
  13. Garraffo R., Dellamonica P., Bernard E., Etesse H., Lapalus P. Steady-state serum pharmacokinetics and bioequivalence of 500 mg oral versus 200 mg intravenous ciprofloxacin. Int J Clin Pharmacol Res. 1989;9(1):29–35. [PubMed] [Google Scholar]
  14. 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]
  15. Höffken G., Lode H., Prinzing C., Borner K., Koeppe P. Pharmacokinetics of ciprofloxacin after oral and parenteral administration. Antimicrob Agents Chemother. 1985 Mar;27(3):375–379. doi: 10.1128/aac.27.3.375. [DOI] [PMC free article] [PubMed] [Google Scholar]
  16. Höffler D., Dalhoff A., Gau W., Beermann D., Michl A. Dose- and sex-independent disposition of ciprofloxacin. Eur J Clin Microbiol. 1984 Aug;3(4):363–366. doi: 10.1007/BF01977496. [DOI] [PubMed] [Google Scholar]
  17. Ledergerber B., Bettex J. D., Joos B., Flepp M., Lüthy R. Effect of standard breakfast on drug absorption and multiple-dose pharmacokinetics of ciprofloxacin. Antimicrob Agents Chemother. 1985 Mar;27(3):350–352. doi: 10.1128/aac.27.3.350. [DOI] [PMC free article] [PubMed] [Google Scholar]
  18. Taburet A. M., Steimer J. L., Doucet D., Singlas E. Le temps de présence moyen dans l'organisme. Un nouveau paramètre pharmacocinétique?. Therapie. 1986 Jan-Feb;41(1):1–10. [PubMed] [Google Scholar]
  19. Vance-Bryan K., Guay D. R., Rotschafer J. C. Clinical pharmacokinetics of ciprofloxacin. Clin Pharmacokinet. 1990 Dec;19(6):434–461. doi: 10.2165/00003088-199019060-00003. [DOI] [PubMed] [Google Scholar]
  20. Weber A., Smith A. L., Wong K., Painter B., Krol G. Comparison of ciprofloxacin assays. Methods Find Exp Clin Pharmacol. 1988 Feb;10(2):123–127. [PubMed] [Google Scholar]
  21. Wingender W., Graefe K. H., Gau W., Förster D., Beermann D., Schacht P. Pharmacokinetics of ciprofloxacin after oral and intravenous administration in healthy volunteers. Eur J Clin Microbiol. 1984 Aug;3(4):355–359. doi: 10.1007/BF01977494. [DOI] [PubMed] [Google Scholar]
  22. Wise R., Andrews J. M., Edwards L. J. In vitro activity of Bay 09867, a new quinoline derivative, compared with those of other antimicrobial agents. Antimicrob Agents Chemother. 1983 Apr;23(4):559–564. doi: 10.1128/aac.23.4.559. [DOI] [PMC free article] [PubMed] [Google Scholar]
  23. Wise R., Lockley R. M., Webberly M., Dent J. Pharmacokinetics of intravenously administered ciprofloxacin. Antimicrob Agents Chemother. 1984 Aug;26(2):208–210. doi: 10.1128/aac.26.2.208. [DOI] [PMC free article] [PubMed] [Google Scholar]

Articles from Antimicrobial Agents and Chemotherapy are provided here courtesy of American Society for Microbiology (ASM)

RESOURCES