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Clinical Pharmacokinetics

, Volume 22, Supplement 1, pp 1–11 | Cite as

The Quinolones

An Overview of their Pharmacology
  • Andrew Fitton
Article

Summary

The fluoroquinolones represent a relatively new class of antibiotics with outstanding therapeutic potential, attributable to their broad spectrum of antimicrobial activity and favourable tissue distribution. They are highly active against most Gram-negative pathogens, as well as Staphylococcus aureus and coagulase-negative staphylococci. In addition, the fluoroquinolones have useful pharmacokinetic properties: they are orally active, and their lipophilicity and low degree of plasma protein binding allow for excellent tissue penetration and concentrations, as reflected in their particularly large apparent volumes of distribution.

Infections due to aerobic Gram-negative pathogens are considered those most susceptible to the quinolones. Disease indications in which these agents appear to offer the greatest therapeutic advantage over currently available alternatives include the following: complicated urinary tract infections (particularly those caused by Pseudomonas aeruginosa or resistant Gram-negative microorganisms); suspected bacterial gastroenteritis; eradication of Salmonella typhi from the faeces in known carriers; P. aeruginosa-associated respiratory exacerbation in patients with cystic fibrosis; and chronic Gram-negative bacterial osteomyelitis.

Direct comparisons of the various quinolones are too limited to date to provide clear therapeutic options. Nevertheless, this class of compounds is likely to play a major role in providing effective oral therapy for conditions that have previously required prolonged parenteral treatment.

Keywords

Fluoroquinolones Ofloxacin Norfloxacin Chlamydia Trachomatis Antimicrobial Chemotherapy 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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References

  1. Baldwin DR, Wise R, Andrews JM, Honeybourne D. The bronchoalveolar distribution of temafloxacin. Thorax 46: 303P, 1991CrossRefGoogle Scholar
  2. Batteiger BE, Jones RB, White A. Efficacy and safety of ofloxacin in the treatment of nongonococcal sexually transmitted disease. American Journal of Medicine 87 (Suppl 6C): 75S–77S, 1989PubMedGoogle Scholar
  3. Bayer AS. Clinical utility of new quinolones in treatment of osteomyelitis and lower respiratory tract infections. European Journal of Clinical Microbiology and Infectious Diseases 8: 1102–1110, 1989CrossRefGoogle Scholar
  4. Black JR, Long JM, Zwicki BE, et al. Multicenter randomized study of a single-dose ofloxacin versus amoxicillin-probenecid for treatment of uncomplicated gonococcal infection. Antimicrobial Agents and Chemotherapy 33: 167–170, 1989PubMedCrossRefGoogle Scholar
  5. Block JM, Walstad RA, Bjertnaes A, et al. Ofloxacin versus trimethoprim-sulfamethoxazole in acute cystitis. Drugs 34 (Suppl. 1): 100–106, 1987PubMedCrossRefGoogle Scholar
  6. Bowie WR, Willetts V, Sibau L. Failure of norfloxacin to eradicate Chlamydia trachomatis in nongonococcal urethritis. Antimicrobial Agents and Chemotherapy 30: 594–597, 1986PubMedCrossRefGoogle Scholar
  7. Campoli-Richards DM, Monk JP, Price A, Benfield P, Todd PA, et al. Ciprofloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs 35: 373–447, 1988PubMedCrossRefGoogle Scholar
  8. Christ W. Central nervous system toxicity of quinolones: human and animal findings. Journal of Antimicrobial Chemotherapy 26 (Suppl. B): 219–225, 1990PubMedCrossRefGoogle Scholar
  9. Christ W, Lehnert T, Ulhrich B. Specific toxicologic aspects of the quinolones. Reviews of Infectious Diseases 10 (Suppl. 1): 141–146, 1988CrossRefGoogle Scholar
  10. Covino JM, Cummings M, Smith B, Benes S, Draft K, et al. Comparison of ofloxacin and ceftriaxone in the treatment of uncomplicated gonorrhea caused by penicillinase-producing and non-penicillinase-producing agents. Antimicrobial Agents and Chemotherapy 34: 148–149, 1990PubMedCrossRefGoogle Scholar
  11. Cruciani M, Concia E, Navarra A, et al. Prophylactic co-trimoxazole versus norfloxacin in neutropenic children — perspective randomized study. Infection 17: 65–69, 1989PubMedCrossRefGoogle Scholar
  12. Davies BI, Maesen FPV. Drug interactions with quinolones. Reviews of Infectious Diseases 11 (Suppl. 5): 1083–1090, 1989CrossRefGoogle Scholar
  13. Drancourt M, Gallais H, Raoult D, Estrangin E, Mallet MN, et al. Ofloxacin penetration into cerebrospinal fluid. Journal of Antimicrobial Chemotherapy 22: 263–265, 1988PubMedCrossRefGoogle Scholar
  14. DuPont HL, Corrado ML, Sabbaj J. The use of norfloxacin in the treatment of acute diarrheal disease. American Journal of Medicine 82: 70–74, 1987CrossRefGoogle Scholar
  15. Ericsson CD, Johnson PC, DuPont HL, Morgan DR, Bitsura AM, et al. Ciprofloxacin or trimethoprim-sulfamethoxazole as initial therapy for travelers’ diarrhea: a placebo-controlled, randomized trial. Annals of Internal Medicine 106: 216–220, 1987PubMedGoogle Scholar
  16. Fillastre JP, Leroy A, Moulin B, Dhib M, Borsa-Lebas F, et al. Pharmacokinetics of quinolones in renal insufficiency. Journal of Antimicrobial Chemotherapy 26 (Suppl. B): 51–60, 1990PubMedCrossRefGoogle Scholar
  17. Fong IW, Linton W, Simbul M, et al. Treatment of nongonococcal urethritis with ciprofloxacin. American Journal of Medicine 82 (Suppl. 4A): 311–316, 1987PubMedGoogle Scholar
  18. Fornara P, Schollmayer E, Seelmann R, Mahr G, Muth P, et al. Penetration of temafloxacin into prostatic tissue. In Rubinstein E (Ed.) Temafloxacin. Proceedings of the 3rd International Symposium on New Quinolones, Vancouver, Canada, July 12–14, 1990. European Journal of Clinical Microbiology and Infectious Diseases, pp. 27–29, 1991Google Scholar
  19. Gerding DN, Hitt JA. Tissue penetration of the new quinolones in humans. Reviews of Infectious Diseases 11 (Suppl. 5): 1046–1057, 1989CrossRefGoogle Scholar
  20. Gonzalez JP, Henwood JM. Pefloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs 37: 628–668, 1989PubMedCrossRefGoogle Scholar
  21. Granneman GR, Carpentier P, Morrison PJ, Pernet AG. Pharmacokinetics of temafloxacin in humans after single oral doses. Antimicrobial Agents and Chemotherapy 35: 436–441, 1991PubMedCrossRefGoogle Scholar
  22. Granneman GR, Mahr G, Locke C, Nickel P, Kirch W, et al. Pharmacokinetics of temafloxacin in patients with liver impairment. Clinical Pharmacokinetics 22 (Suppl. 1): 24–32, 1992aPubMedCrossRefGoogle Scholar
  23. Granneman GR, Stephan U, Birner B, Sörgel F, Mukherjee D. Effect of antacid medication on the pharmacokinetics of temafloxacin. Clinical Pharmacokinetics 22 (Suppl. 1): 83–89, 1992bPubMedCrossRefGoogle Scholar
  24. Halkin H. Adverse effects of the fluoroquinolones. Review of Infectious Diseases 10 (Suppl. 1): S258–S261, 1988CrossRefGoogle Scholar
  25. Henry NK, Schultz HJ, Grubbs NC, Muller SM, Ilstrup DM, et al. Comparison of ciprofloxacin and co-trimoxazole in the treatment of uncomplicated urinary tract infections in women. Journal of Antimicrobial Chemotherapy 18 (Suppl. D): 103–106, 1986PubMedGoogle Scholar
  26. Henwood JM, Monk JP. Enoxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs 36: 32–66, 1988PubMedCrossRefGoogle Scholar
  27. Hodson ME, Roberts CM, Butland RJA, Smith MJ, Batten JC. Oral ciprofloxacin compared with conventional intravenous treatment for Pseudomonas aeruginosa infection in adults with cystic fibrosis. Lancet 1: 235–237, 1987PubMedCrossRefGoogle Scholar
  28. Hooper DC, Wolfson JS. Treatment of genitourinary tract infections with fluoroquinolones: clinical efficacy in genital infections and adverse effects. Antimicrobial Agents and Chemotherapy 33: 1662–1667, 1989PubMedCrossRefGoogle Scholar
  29. Hooper DC, Wolfson JS. Fluoroquinolone antimicrobial agents. New England Journal of Medicine 324: 384–394, 1991PubMedCrossRefGoogle Scholar
  30. Iravani A. Comparative, double-blind, prospective multicenter trial of temafloxacin versus trimethoprim-sulfamethoxazole in uncomplicated urinary tract infections in women. Antimicrobial Agents and Chemotherapy 35: 1777–1781, 1991PubMedCrossRefGoogle Scholar
  31. Janknegt R. Drug interactions with quinolones. Journal of Antimicrobial Chemotherapy 26 (Suppl. D): 7–29, 1990PubMedCrossRefGoogle Scholar
  32. Jensen T, Pedersen SS, Høiby N, Koch C. Efficacy of oral fluoroquinolones versus conventional intravenous antipseudomonal chemotherapy in treatment of cystic fibrosis. European Journal of Clinical Microbiology 6: 618–622, 1987PubMedCrossRefGoogle Scholar
  33. Liang RHS, Yung RWH, Chan T-K, et al. Ofloxacin versus cotrimoxazole for prevention of infection in neutropenic patients following cytotoxic chemotherapy. Antimicrobial Agents and Chemotherapy 34: 215–218, 1990PubMedCrossRefGoogle Scholar
  34. Malmverni R, Glauser MP. Comparative studies of fluoroquinolones in the treatment of urinary tract infections. Review of Infectious Diseases 10 (Suppl. 1): 153–163, 1988CrossRefGoogle Scholar
  35. Maple P, Brumfitt W, Hamilton-Miller JMT. A review of the antimicrobial activity of the fluoroquinolones. Journal of Chemotherapy 2: 280–294, 1990PubMedGoogle Scholar
  36. Monk JP, Campoli-Richards DM. Ofloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs 33: 346–391, 1987PubMedCrossRefGoogle Scholar
  37. Nayagam AT, Ridgeway GL, Oril JD. Efficacy of ofloxacin. The treatment of non-gonococcal urethritis in men and genital infections caused by Chlamydia trachomatis in men and women. Journal of Antimicrobial Chemotherapy 22 (Suppl. C): 155–158, 1988PubMedGoogle Scholar
  38. Neu HC. The quinolones. Infectious Disease Clinics of North America 3: 625–639, 1989PubMedGoogle Scholar
  39. Neuman M. Clinical pharmacokinetics of the newer antibacterial 4-quinolones. Clinical Pharmacokinetics 14: 96–121, 1988PubMedCrossRefGoogle Scholar
  40. Norrby SR, Ljungberg B. Pharmacokinetics of fluorinated 4-quinolones in the aged. Reviews of Infectious Diseases 11 (Suppl. 5): 1102–1106, 1989CrossRefGoogle Scholar
  41. Rademaker CM, Hoepelman IM, Wolfhagen MJ, Beumer H, Rozenberg-Arska M, et al. Results of a double-blind placebocontrolled study using ciprofloxacin for prevention of travelers’ diarrhea. European Journal of Clinical Microbiology and Infectious Diseases 8: 690–694, 1989CrossRefGoogle Scholar
  42. Sabbaj J, Hoagland VL, Cook T. Norfloxacin versus co-trimoxazole in the treatment of recurring urinary tract infections in men. Scandinavian Journal of Infectious Diseases 48 (Suppl.): 48–53, 1986PubMedGoogle Scholar
  43. Scott DA, Haberberger RL, Thornton SA, Hyams KC. Norfloxacin for the prophylaxis of travelers’ diarrhea in U.S. military personnel. American Journal of Tropical Medicine and Hygiene 42: 160–164, 1990PubMedGoogle Scholar
  44. Scully BE, Nakatomi M, Ores C, et al. Ciprofloxacin therapy in cystic fibrosis. American Journal of Medicine 82 (Suppl. 4A): 196–201, 1987PubMedGoogle Scholar
  45. Sörgel F. Penetration of temafloxacin into body tissues and fluids. Clinical Pharmacokinetics 22 (Suppl. 1): 57–63, 1992PubMedCrossRefGoogle Scholar
  46. Sörgel F, Granneman GR, Stephan U, Locke C. Effects of cimetidine on the pharmacokinetics of temafloxacin. Clinical Pharmacokinetics 22 (Suppl. 1): 75–82, 1992aPubMedCrossRefGoogle Scholar
  47. Sörgel F, Mahr G, Granneman GR, Stephan U. Effects of two quinolone antibacterials, temafloxacin and enoxacin, on theophylline pharmacokinetics. Clinical Pharmacokinetics 22 (Suppl. 1): 65–74, 1992bPubMedCrossRefGoogle Scholar
  48. Stahlmann R. Safety profile of the quinolones. Journal of Antimicrobial Chemotherapy 26 (Suppl. D): 31–44, 1990PubMedCrossRefGoogle Scholar
  49. Urinary Tract Infection Study Group. Coordinated multicenter study of norfloxacin versus trimethoprim-sulfamethoxazole treatment of symptomatic urinary tract infections. Journal of Infectious Diseases 155: 170–177, 1987CrossRefGoogle Scholar
  50. Vergin H, Metz R. Review of developments in fluoroquinolones. Drugs of Today 27: 177–192, 1991Google Scholar
  51. Waldvogel FA. Clinical role of the quinolones today and in the future. European Journal of Clinical Microbiology and Infectious Diseases 8: 1075–1079, 1989CrossRefGoogle Scholar
  52. Weidner W, Schiefer HG, Dalhoff A. Treatment of chronic bacterial prostatitis with ciprofloxacin: results of a one-year follow-up study. American Journal of Medicine 82: 280–283, 1987PubMedGoogle Scholar
  53. Wijnands GJA, Vree TB, Janssen TJ, Guelen PJM. Drug-drug interactions affecting fluoroquinolones. American Journal of Medicine 87 (Suppl. 6C): 47–51, 1989Google Scholar
  54. Winston DJ, Ho WG, Bruckner DA, Gale RP, Champlin RE. Ofloxacin versus vancomycin/polymyxin for prevention of infections in granulocytopenic patients. American Journal of Medicine 88: 36–42, 1990PubMedCrossRefGoogle Scholar
  55. Wiström J, Jertborn M, Hedström SA, et al. Short-term self-treatment of travellers’ diarrhoea with norfloxacin: a placebo-controlled study. Journal of Antimicrobial Chemotherapy 23: 905–913, 1989PubMedCrossRefGoogle Scholar
  56. Wiström J, Norrby SR, Burman LG, Lundholm R, Jellheden B, et al. Norfloxacin versus placebo for prophylaxis against traveller’s diarrhoea. Journal of Antimicrobial Chemotherapy 20: 563–574, 1987PubMedCrossRefGoogle Scholar
  57. Wolfson JS. Quinolone antimicrobial agents: adverse effects and bacterial resistance. European Journal of Clinical Microbiology and Infectious Diseases 8: 1080–1092, 1989CrossRefGoogle Scholar
  58. Wolfson JS, Hooper DC. Treatment of genitourinary tract infections with fluoroquinolones: activity in vitro, pharmacokinetics, and clinical efficacy in urinary tract infections and prostatitis. Antimicrobial Agents and Chemotherapy 33: 1655–1661, 1989aPubMedCrossRefGoogle Scholar
  59. Wolfson JS, Hooper DC. Fluoroquinolone antimicrobial agents. Clinical Microbiology Reviews 2: 378–424, 1989bPubMedGoogle Scholar

Copyright information

© Adis International Limited 1992

Authors and Affiliations

  • Andrew Fitton
    • 1
  1. 1.Adis Drug Information ServicesAucklandNew Zealand

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