Pharmaceutisch Weekblad

, Volume 8, Issue 1, pp 67–71 | Cite as

Quinolones and colonization resistance in human volunteers

  • J. J. M. Van Saene
  • H. K. F. Van Saene
  • J. N. Geitz
  • N. J. P. H. Tarko-Smit
  • C. F. Lerk
Quinolones in Perspective


The suppression of alimentary canal flora by the three quinolones nalidixic acid, ciprofloxacin and pefloxacin was investigated in fifteen volunteers. They received the three quinolone compounds in tablet form both uncoated and colon-coated.Escherichia coli suppression was poor under nalidixic acid, but complete under ciprofloxacin and pefloxacin for both administration forms. The indigenous anaerobic flora contributing to the control of aerobicStreptococcus faecalis andCandida albicans in the intestines ('colonization resistance') was not affected by nalidixic acid and pefloxacin, and only slightly by ciprofloxacin. Out of the three quinolone compounds, only colon-coated pefloxacin was associated with a considerable absorption rate at colonie level. Using these criteria of successfulEscherichia coli clearing from the intestinal canal - left the indigenous flora more or less intact (in a 'selective' way) - and a good absorption rate, pefloxacin is found to be superior to ciprofloxacin and nalidixic acid. These results suggest that a colon-coated tablet with a low dose of pefloxacin is a promising administration form in the therapy of recurrent urinary tract infections and diarrhoeal diseases and in the prevention of gut colonization in immunocompromised hosts.

Key words

Ciprofloxacin Colonization resistance Enterobacteriaceae Intestinal decontamination Nalidixic acid Pefloxacin 


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. 1.
    Van der Waay D, Berghuis-de Vries HM, Lekkerkerk-van der Wees JEC. Colonization resistance of the digestive tract in conventional and antibiotic-treated mice. J Hyg (Camb) 1971;69:405-n.Google Scholar
  2. 2.
    Van Saene HKF, Stoutenbeek ChP, Miranda DR, Zandstra DF. A novel approach to infection control in the intensive care unit. Acta Anaesthesiol Belg 1983;34:193–208.Google Scholar
  3. 3.
    Shannon KP, Phillips I. The antimicrobial spectrum of the quinolones. Res Clin Forums 1985;7:29–36.Google Scholar
  4. 4.
    Fass RJ. The quinolones. Ann Intern Med 1985;102:400–2.Google Scholar
  5. 5.
    Klinge E, Männisto PT, Mäntylä J, Hänninen U. Single- and multiple-dose pharmacokinetics of pipemidic acid in normal human volunteers. Antimicrob Agents Chemother 1984;26:69–73.Google Scholar
  6. 6.
    Kucers A, Bennet NMcK. The use of antibiotics. London: William Heinemann, 1979:734.Google Scholar
  7. 7.
    Monteay G, Goueffon Y, Roquet F. Absorption, distribution, metabolic fate and elimination of pefloxacin mesylate in mice, rats, dogs, monkeys and humans. Antimicrob Agents Chemother 1984;25:463–72.Google Scholar
  8. 8.
    Brumfitt W, Franklin I, Grady D, Hamilton-Miller JMT, Iliffe A. Changes in the pharmacokinetics of ciprofloxacin and faecal flora during administration of a seven day course to human volunteers. Antimicrob Agents Chemother 1984;26:757–61.Google Scholar
  9. 9.
    Wade JC, De Jongh CA, Newman KA, Crowley J, Wiernik PH, Schimpff SC. Selective antimicrobial modulation as prophylaxis against infection during granulocytopenia: trimethoprim-sulfamethoxazole vs. nalidixic acid. J Infect Dis 1983;147:624–34.Google Scholar
  10. 10.
    Sleijfer DTh, Mulder NH, De Vries-Hospers HG, et al. Infection prevention in granulocytopenic patients by selective decontamination of the digestive tract. Eur J Cancer 1980;16:859–69.Google Scholar
  11. 11.
    Stamey TA, Timothy M, Miller M, Mihara G. Recurrent urinary infections in adult women. The role of enterobacteria. Calif Med 1971;115:1–19.Google Scholar
  12. 12.
    Preitsakis JK, Thompson L, Harding GKM, Marrie TJ, Hoban S, Ronald AR. A comparison of the efficacy of nalidixic acid and cefalexin in bacteriuric women and their effect on faecal and periuretral carriage of Enterobacteriaceae. J Infect Dis 1981;143:603–8.Google Scholar
  13. 13.
    Ronald AR, Harding GKM, Mathias R, Wong CK, Muir P. Prophylaxis of recurring urinary tract infection in females: a comparison of nitrofurantoin with trimethoprim-sulfamethoxazole. Can Med Assoc J 1975;112S:13–6.Google Scholar
  14. 14.
    Hoshimoto J, Akao M, Amano F. Fundamental and clinical study of AT 2266 in intestinal tract infection. Chemotherapy 1984;32(S3):630–1.Google Scholar
  15. 15.
    Schimpff SC, Young UM, Greene WH, Vermeulen GD, Moody MR, Wiernik PH. Origin of infection in acute non-lymphocytic leukemia. Ann Intern Med 1972;77:707–14.Google Scholar
  16. 16.
    Rozenberg-Arska M, Dekker AW, Verhoef J. Ciprofloxacin for selective decontamination of the alimentary tract in patients with acute leukemia during remission induction treatment: the effect on fecal flora. J Infect Dis 1985;152:104–7.Google Scholar

Copyright information

© Royal Dutch Association for Advancement of Pharmacy 1986

Authors and Affiliations

  • J. J. M. Van Saene
    • 1
  • H. K. F. Van Saene
    • 1
  • J. N. Geitz
    • 1
  • N. J. P. H. Tarko-Smit
    • 1
  • C. F. Lerk
    • 1
  1. 1.Department of Pharmaceutical Technology and DispensingState University of GroningenAW GroningenThe Netherlands

Personalised recommendations