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Pharmacokinetic Disposition of Quinolones in Human Body Fluids and Tissues

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Summary

The unique pharmacokinetic properties as well as the body fluid and tissue penetration of quinolones are discussed.

Quinolones are well absorbed from the gastrointestinal tract and are eliminated with considerable differences in their terminal half-lives. The major elimination pathways of quinolones are renal excretion and hepatic metabolism. Renally, these drugs undergo the potential excretion mechanisms (glomerular filtration, tubular secretion, reabsorption). In the liver, they are metabolised primarily by oxidation as well as by conjugative pathways. However, the metabolic pattern and extent of metabolism differ significantly between individual agents.

Alterations in the pharmacokinetic disposition of these agents in liver and renal failure as well as in elderly patients are observed as predicted from their excretion pattern. In addition, quinolones can interact with a number of other compounds at hepatic (e.g. with xanthine derivatives), renal (with probenecid) and gastrointestinal (with antacids) sites.

The volume of distribution of quinolones is considerably higher than body volume, which suggests intracellular penetration. Studies on tissue penetration show that concentrations exceeding plasma levels are obtained in most tissues. The highest tissue/plasma concentration ratios are achieved in lung and kidney, whereas concentrations in fat are considerably lower than in plasma.

Body fluid penetration is introduced as a new approach to evaluate distribution kinetics of quinolones. With the exception of those in nasal secretions and ejaculate, body fluid levels of these drugs rarely reach plasma levels. The body fluid penetration model allows for differentiation among individual agents. There is no apparent relationship between differences in body fluid penetration of quinolones and differences in volume of distribution. For the clinical use of these drugs it is important that the concentrations achieved in body fluids and tissues are sufficient to kill most pathogens. A discussion on the relationship between plasma and tissue levels and the MICs of quinolones is, however, beyond the scope of this article.

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References

  • Adam D, Heilmann HD, Weismeier K. Concentrations of ticarcillin and clavulanic acid in human bone after prophylactic administration of 5.2 g of timentin. Antimicrobial Agents and Chemotherapy 31: 935–939, 1987

    Article  PubMed  CAS  Google Scholar 

  • Austgen M, Morgenroth A, Seelmann R, Muth P, Sörgel F. Pharmacokinetics and pleural penetration of ciprofloxacin in patients with empyema thoracis. 6th Mediterranean Congress of Chemotherapy, Taormina, May 22–27, 1988. Abstract no. 124, p. 222. 1988

  • Bassaris HP, Papadakis N, Gogos C, Siamplis D. Penetration of ciprofloxacin into human cerebrospinal fluid. In Neu & Weuta (Eds) Proceedings of the 1st International Ciprofloxacin Workshop, Leverkusen. Nov. 6–8, 1985, pp. 204–205, Excerpta Medica, Amsterdam 1986

    Google Scholar 

  • Bergeron MG, Brousseau L. Tissue fluid pharmacokinetic models in humans and animals. In Zak O, Sande MA (Eds) Experimental models in antimicrobial chemotherapy, Vol. 1, pp. 71–107, Academic Press, London, 1986

    Google Scholar 

  • Bergeron MG, Thabet M, Roy R, Lessard C, Foncault P. Norfloxacin penetration into human renal and prostatic tissue after oral administration. Antimicrobial Agents and Chemotherapy 28: 349–350, 1985

    Article  PubMed  CAS  Google Scholar 

  • Boerema JBJ, Dalhoff A, Debruyne FMY. Ciprofloxacin distribution in prostatic tissue and fluid following oral administration. Chemotherapy 31: 13–18, 1985

    Article  PubMed  CAS  Google Scholar 

  • Bolcskei P, Burkhardt G, Klatt O, Thoma B, Gill E. Penetration of ciprofloxacin in the pleural fluid. Proceedings of the 5th Mediterranean Congress of Chemotherapy, Cairo, Oct. 26–Nov. 1, 1986, pp. 290–292, 1987

  • Brandt R, Meyer J. The in vitro protein binding of Ro 23-6240 (AM 833) in human, dog and rat plasma. Roche Research Report no. B-104′181, 1985

  • Braun R, Dürig M. Penetration of ciprofloxacin into human bone tissue. In Neu & Weuta (Eds) Proceedings of the 1st International Ciprofloxacin Workshop, Leverkusen, Nov. 6–8, 1985, pp. 197–200, Excerpta Medica, Amsterdam, 1986

    Google Scholar 

  • Brion N, Lessana A, Mosset F, Lefevre JJ, Montay G. Penetration of pefloxacin in human heart valves. Journal of Antimicrobial Chemotherapy 17 (Suppl. B): 89–92, 1986

    Article  PubMed  Google Scholar 

  • Chang T, Black A, Dunky A, Wolf R, Sedman A, et al. Pharmacokinetics of intravenous and oral enoxacin in healthy volunteers. Journal of Antimicrobial Chemotherapy 21 (Suppl. B): 49–56, 1988

    Article  PubMed  CAS  Google Scholar 

  • Couraud L, Fourtillan JB, Saux MC, Bryskier A, Vincent du Laurier M. Diffusion of ofloxacin into human lung tissue. Proceedings of the 14th International Congress of Chemotherapy, Kyoto, 1985, pp. 1795–1796, 1985

  • Dalhoff A, Aigner KR, Eickenberg HU. Penetration activities of ciprofloxacin into muscle, skin and fat following oral administration. Proceedings of the 5th Mediterranean Congress of Chemotherapy, Cairo, Oct 26–Nov 1, 1986, pp. 294–295, 1987

  • Daschner FD, Westenfelder M, Dalhoff A. Penetration of ciprofloxacin into kidney, fat, muscle and skin tissue. European Journal of Clinical Microbiology 5: 212–213, 1986

    Article  PubMed  CAS  Google Scholar 

  • Davies BI, Maesen FPV, Teengs JP, Baur C. The quinolones in chronic bronchitis. Pharmaceutisch Weekblad 8: 53–59, 1986

    Article  CAS  Google Scholar 

  • Davis RL, Koup JR, Williams-Warren J, Weber A. Smith AL. Pharmacokinetics of three oral formulations of ciprofloxacin. Antimicrobial Agents and Chemotherapy 28: 74–77, 1985

    Article  PubMed  CAS  Google Scholar 

  • Dcllamonica P, Bernard E, Etesse H, Garraffo R. The diffusion of pefloxacin into bone and the treatment of osteomyelitis. Journal of Antimicrobial Chemotherapy 17 (Suppl. B): 93–102, 1986

    Article  Google Scholar 

  • Dow J, Chazal J, Frydman AM, Janny P, Woehrle R, et al. Transfer kinetics of pefloxacin into cerebro-spinal fluid after one hour i.v. infusion of 400mg in man. Journal of Antimicrobial Chemotherapy 17 (Suppl. B): 81–87, 1986

    Article  PubMed  Google Scholar 

  • Drusano GL, Standiford HC, Plaisance K, Forrest A, Leslie J. et al. Absolute oral bioavailability of ciprofloxacin. Antimicrobial Agents and Chemotherapy 30: 444–446, 1986

    Article  PubMed  CAS  Google Scholar 

  • Easmon CSF, Crane JP. Uptake of ciprofloxacin by human neutrophils. Journal of Antimicrobial Chemotherapy 16: 67–73, 1985

    Article  PubMed  CAS  Google Scholar 

  • Eickenberg HU, Dalhoff A. Tissue distribution of ciprofloxacin following oral and intravenous administration. Proceedings of the 14th International Congress of Chemotherapy, Kyoto, 1985, pp. 1612–1613, 1985

  • Flor S, Guay D, Tack K, Beals B, Weintraub H, et al. Evaluation of the interaction and safety of administration of antacids with ofloxacin. International Congress for Infectious Diseases, Rio de Janeiro, April 17–21, 1988. Abstract no. 706, p. 233, 1988

  • Fong IW, Ledbetter W, Vandenbroucke A, Simbul W, Rahm V. Penetration of ciprofloxacin after single doses in normal and infected bones. In Neu & Weuta (Eds) Proceedings of the 1st International Ciprofloxacin Workshop, Leverkusen, Nov 6–8, 1985, pp. 201–203, Excerpta Medica, Amsterdam, 1986

    Google Scholar 

  • Fong IW, Vandenbroucke A, Simbul M. Penetration of enoxacin into bronchial secretions. Antimicrobial Agents and Chemotherapy 31: 748–751, 1987a

    Article  PubMed  CAS  Google Scholar 

  • Fong IW, Rittenhouse D, Simbul M, Vandenbroucke A. Bone penetration of enoxacin after oral and intravenous dosing. 15th International Congress of Chemotherapy, Istanbul, July 19–24, 1987, abstract no. 1197, p. 325, 1987b

  • Ganong WF. Review of medical physiology. 10th ed., pp. 344–345, Lange Medical Publications, Los Altos, 1981

    Google Scholar 

  • Gibaldi M. Biopharmaceutics and clinical pharmacokinetics, 3rd ed., pp. 169–170, Lea & Febiger, Philadelphia, 1984

    Google Scholar 

  • Giebel W, Schönleber KH, Breuninger H, Ullmann U. Quantitative Bestimmung von Protein, Albumin und Antibiotika im Nasensekret gesunder Probanden. Archives of Oto-Rhino-Laryngology 225: 149–159, 1979

    Article  PubMed  CAS  Google Scholar 

  • Granneman GR, Snyder KM, Shu VS. Difloxacin metabolism and pharmacokinetics in humans after single oral doses. Antimicrobial Agents and Chemotherapy 30: 689–693, 1986

    Article  PubMed  CAS  Google Scholar 

  • Gruber G, Jaehde U, Sörgel F, Heiss R, Schunack W. Relationships between the chemical structure and the HPLC capacity factor of gyrase inhibitors and their metabolites in different methanol-water eluents. Fresenius’ Zeitschrift für Analytische Chemie 330: 388–389, 1988

    Article  Google Scholar 

  • Höffken G, Lode H, Prinzing C, Borner K, Koeppe P. Pharmacokinetics of ciprofloxacin after oral and parenteral administration. Antimicrobial Agents and Chemotherapy 27: 375–379, 1985

    Article  PubMed  Google Scholar 

  • Höffken G, Lode H, Wiley R, Glatzel TD, Sievers B, et al. Pharmacokinetics and bioavailability of ciprofloxacin and ofloxacin: effect of food and antacid intake. Reviews of Infectious Diseases 10 (Suppl. 1): S138–S139, 1988

    Google Scholar 

  • Jaehde U, Sörgel F, Schunack W. Influence of lipophilicity on pharmacokinetics of quinolones. 71st Annual Meeting of FASEB, Washington, DC, March 29–April 2, 1987. Abstract no. 3224, 1987a

  • Jaehde U, Sörgel F, Gottschalk B, Stephan U, Schunack W. Reduced bioavailability of pefloxacin after coadministration with antacids. 1st Biennial Conference on Chemotherapy of Infectious Diseases and Malignancies, Munich, April 26–29, 1987. Abstract no. 280, 1987b

  • Jaehde U, Sörgel F, Gottschalk B, Stephan U, Schunack W. Pharmacokinetics of pefloxacin and metronidazole after concomitant administration. 1st Biennial Conference on Chemotherapy of Infectious Diseases and Malignancies, Munich, April 26–29, 1987. Abstract no. 278, 1987c

  • Jaehde U, Malter U, Sörgel F, Gottschalk B, Wiesemann H, et al. Individual factors affecting the pharmacokinetics of pefloxacin. Proceedings of the 15th International Congress of Chemotherapy, Istanbul, July 19–24, 1987. In Berkarda & Kuemmerle (Eds) Progress in antimicrobial and anticancer chemotherapy, Vol. 1, pp. 883–885, Ecomed-Verlag, Landsberg, 1987d

    Google Scholar 

  • Jaehde U, Zürcher J, Sörgel F, Naber K, Sigl G, et al. Comparative bioavailability and pharmacokinetics of ciprofloxacin and pefloxacin in healthy volunteers. 2nd International Symposium on New Quinolones, Geneva, August 25–27, 1988. Abstract no. 80, 1988a

  • Jaehde U, Sörgel F, Naber K, Schumacher H, Kraus C, et al. Distribution of ciprofloxacin into various body fluids of healthy volunteers. 6th Mediterranean Congress of Chemotherapy, May 22–27, Taormina, 1988. Abstract no. 340, p. 160, 1988b

  • Jaehde U, Mahr G, Zürcher J, Naber K, Schunack W, et al. Absolute bioavailability (F), distribution and metabolism of enoxacin in healthy volunteers. 89th Annual Meeting ASCPT, San Diego, March 9–11, 1988. Abstract PII 6-7, Clinical Pharmacology and Therapeutics 43: 157, 1988c

    Google Scholar 

  • Jaehde U, Zürcher J, Sörgel F, Naber K, Schunack W. Metabolism of ciprofloxacin in man following oral and intravenous administration. 2nd International Symposium on New Quinolones, Geneva, August 25–27, 1988. Abstract no. 145, 1988d

  • Junqueira LC, Carneiro J. Basic histology, 3rd ed., Lange Medical Publications, Los Altos, 1980

    Google Scholar 

  • Kalager T, Digranes A, Bergan T, Rolstad T, Ishigam J. Pharmacokinetics of ofloxacin in serum and skin blister. Proceedings of the 14th International Congress of Chemotherapy, Kyoto, 1985, pp. 1765–1766, 1985

  • Kitzes-Cohen R, Miler A, Gilboa A, Harel D. Penetration of ciprofloxacin into human cerebrospinal fluid: preliminary results. In Neu & Weuta (Eds) Proceedings of the 1st International Ciprofloxacin Workshop, Leverkusen, Nov 6–8, 1985, pp. 206–208, Excerpta Medica, Amsterdam, 1986

    Google Scholar 

  • Klinge E, Männisto PT, Mäntylä R, Mattila J, Hänninen U. Single- and multiple-dose pharmacokinetics of pipemidic acid in normal human volunteers. Antimicrobial Agents and Chemotherapy 26: 69–73, 1984

    Article  PubMed  CAS  Google Scholar 

  • Kumon H, Mizuno A, Kishi M, Miyata K, Ohmori H. The concentration of ofloxacin in human prostatic tissue and fluid. Proceedings of the 14th International Congress of Chemotherapy, Kyoto, 1985, pp. 1767–1768, 1985

  • LeBel M, Vallee F, Bergeron MG. Tissue penetration of ciprofloxacin after single and multiple doses. Antimicrobial Agents and Chemotherapy 29: 501–505, 1986

    Article  PubMed  CAS  Google Scholar 

  • Lerebours-Pigeonnière G, Gres JJ, Montay G, Bonmarchard G, Dujon A, et al. Diffusion of pefloxacin in lung parenchyma. 15th International Congress of Chemotherapy, Istanbul, July 19–24, 1987. Abstract no. 77, p. 112, 1987

  • Lode H, Hampel B, Wachter T, Borner K, Koeppe P. Single dose pharmacokinetics of fleroxacin in volunteers, after fasting, a standard breakfast, and antacids. 15th International Congress of Chemotherapy, Istanbul, July 19–24, 1987. Workshop on fleroxacin (Ro 23-6240): a new oral oncc-a-day quinolone. Abstract, p. 14, 1987a

    Google Scholar 

  • Lode H, Höfften G, Olschewski P, Sievers B, Kirch A, et al. Pharmacokinetics of ofloxacin after parenteral and oral administration. Antimicrobial Agents and Chemotherapy 31: 1338–1342, 1987b

    Article  PubMed  CAS  Google Scholar 

  • Logemann C, Ohnhaus EE. Enoxacin, a differential inhibitor of the microsomal liver enzyme system in men. 26th Interscience Conference of Antimicrobial Agents and Chemotherapy, New Orleans, 1986. Abstract no. 481, p. 185, 1986

  • Loos U, Schwabe HK, Vogel F. Ofloxacin concentrations in human plasma, bronchial secretions, bronchoalveolar lavage and alveolar macrophages. 15th International Congress of Chemotherapy, Istanbul, July 19–24, 1987. Abstract no. 78, p. 112, 1987

  • Loos U, Marklein G, Scholl H, Hübner U, Kaster H, et al. Bronchopulmonary penetration of ciprofloxacin. 6th Mediterranean Congress of Chemotherapy, Taormina, Italy, May 22–27, 1988. Abstract no. 341, p. 160, 1988

  • Madsen PO, Dørflinger T, Larsen EH, Gasser TC. Pharmacokinetics of antibacterial agents used for treatment of bacterial prostatitis. In Weidner et al. (Eds) Therapy of prostatitis, pp. 17–20, Zuckschwerdt Verlag, München, 1986

    Google Scholar 

  • Mahr G, Sörgel F, Naber K. Body fluid penetration and metabolism of norfloxacin in healthy volunteers using a new metabolite specific assay. Proceedings of the 15th International Congress of Chemotherapy, Istanbul, July 19–24, 1987. In Berkarda & Kuemmerle (Eds) Progress in antimicrobial and anticancer chemotherapy, Vol. 1, pp. 883–885, Ecomed-Verlag, Landsberg, 1987

    Google Scholar 

  • Mahr G, Metz R, Vergin H, Fabian W, Muth P, et al. Metabolism of gyrase inhibitors in perfused rat liver and liver microsomes from different species. 72nd Annual Meeting of FASEB, Las Vegas, May 1–5, 1988. Abstract no. 4414, 1988

  • Malinverni R, Glauser MP. Comparative studies of fluoroquinolones in the treatment of urinary tract infections. Reviews of Infectious Diseases 10 (Suppl. 1): S153–S163, 1988

    Article  PubMed  Google Scholar 

  • Malmborg AS, Rannikko S. Enoxacin distribution in human tissues after multiple oral administration. Journal of Antimicrobial Chemotherapy 21 (Suppl. B): 57–60, 1988

    Article  PubMed  CAS  Google Scholar 

  • Metz R, Sörgel F, Gottschalk B, Stephan U. Pharmacokinetics of pefloxacin alone and in combination with other antimicrobial agents. 1st Biennial Conference on Chemotherapy of Infectious Diseases and Malignancies, April 26–29, Munich, 1987. Abstract no. 277, 1987a

  • Metz R, Sörgel F, Naber K. Pharmacokinetics and body fluid penetration of ofloxacin after multiple dosing in healthy volunteers. Proceedings of the 15th International Congress of Chemotherapy, Istanbul, July 19–24, 1987. In Berkarda & Kuemmerle (Eds) Progress in antimicrobial and anticancer chemotherapy, Vol. 2, pp. 1912–1913, Ecomed-Verlag, Landsberg, 1987b

    Google Scholar 

  • Metz R, Sörgel F, Federspil P, Malter U, Koch HU, et al. Penetration of pefloxacin into saliva, sputum, sweat, tears and nasal secretions. Reviews of Infectious Diseases 10 (Suppl. I): S97, 1988

    Google Scholar 

  • Mizoguchi H, Maeda Y, Shimizu T. An appraisal of ofloxacin level in semen. Proceedings of the 14th International Congress of Chemotherapy, Kyoto, 1985, pp. 1793–1794, 1985

  • Montay G, Goueffon Y, Roquet F. Absorption, distribution, metabolic fate, and elimination of pefloxacin mesylate in mice. rats, dogs, monkeys and humans. Antimicrobial Agents and Chemotherapy 25: 436–472, 1984

    Article  Google Scholar 

  • Naber KG, Sörgel F, Schumacher H, Nausch I, Mahr G. True penetration of quinolones into prostatic fluid of man determined by a new method. 27th Interscience Conference of Antimicrobial Agents and Chemotherapy, October 4–7, New York, 1987. Abstract no. 1270, p. 318, 1987a

  • Naber KG, Sörgel F, Schumacher H, Metz R. In vitro activity of fleroxacin against isolates causing complicated urinary tract infections and concentrations in prostatic fluid in volunteers. 15th International Congress of Chemotherapy, Istanbul, July 19–24, 1987. Workshop on fleroxacin (Ro 23-6240): a new oral once-a-day quinolone. Abstract, p. 13, 1987b

  • Naber KG, Sörgel F, Kees F, Schumacher H, Metz R, et al. Norfloxacin concentrations in prostatic adenoma tissue (patients) and in prostatic fluid in patients and volunteers. 15th International Congress of Chemotherapy, Istanbul, July 19–24, 1987. In Berkarda & Kuemmerle (Eds) Progress in antimicrobial and anticancer chemotherapy, Vol. 2, p. 352, Ecomed-Verlag, Landsberg, 1987c

    Google Scholar 

  • Naber KG, Sörgel F, Schumacher H, Sigl G, Zürcher J, et al. Enoxacin concentrations in prostatic and seminal fluid in volunteers. 2nd International Symposium on New Quinolones, Geneva, August 25–27, 1988. Abstract no. 302, 1988

  • Noel F, Couet W, Lefebvre MA, Akbaraly JP, Mignot A, et al. Diffusion of ofloxacin in human tissues. Proceedings of the 5th Mediterranean Congress of Chemotherapy, Cairo, Oct 26–Nov 1, 1986, pp. 300–301, 1987

  • Ozaki T, Uchida H, Irikura T. Studies on metabolism of AM-715 in humans by high-performance liquid chromatography. Chemotherapy 29: 128–135, 1981

    CAS  Google Scholar 

  • Panneton AC, Bergeron MG, LeBel M. Tissue penetration of fleroxacin after single and multiple 400 and 800 mg dosage regimens. 5th International Congress for Infectious Diseases, Rio de Janeiro, April 17–21, 1988. Abstract no. 416, p. 26, 1988

  • Pfau A, Perlberg S, Shapira A. The pH of the prostatic fluid in health and disease: implications of treatment in chronic bacterial prostatitis. Journal of Urology 119: 384–387, 1978

    PubMed  CAS  Google Scholar 

  • Radtke HJ, Floh W, Böcker R, Hopf G. Distribution of ciprofloxacin in serum, lung and pleural tissue in patients undergoing lung surgery. 15th International Congress of Chemotherapy, Istanbul, July 19–24, 1987. Abstract no. 126, p. 120, 1987

  • Rowland M, Tozer TN. Clinical pharmacokinetics: concepts and applications, pp. 37–38, Lea & Febiger, Philadelphia, 1980

    Google Scholar 

  • Sakamoto H, Sasaki J, Uematsu M, Morihana T, Imoto T, et al. Ofloxacin: its blood level, penetration into saliva and distribution in tooth extraction wound. 15th International Congress of Chemotherapy, Istanbul, July 19–24, 1987. Abstract no. 108, p. 117, 1987

  • Sato K. The physiology, pharmacology and biochemistry of the eccrine sweat gland. Reviews of Physiology, Biochemistry and Pharmacology 79: 51–131, 1977

    Article  PubMed  CAS  Google Scholar 

  • Saux MC, Grellet J, Couraud L, Leng B, Hazane C. Diffusion of enoxacin into human lung tissue. 15th International Congress of Chemotherapy, Istanbul, July 19–24, 1987. Abstract no. 139, p. 123, 1987

  • Schentag JJ, Sedman AJ, Wilton JH, Thomas DJ, Schultz RW, et al. Interactions between enoxacin, ranitidine and antacids. 3rd European Congress of Clinical Microbiology, The Hague, 1987. Abstract, 1987

  • Schlenkhoff D, Knopf J, Dalhoff A. Penetration of ciprofloxacin into human lung tissue. In Neu & Weuta (Eds) Proceedings of the 1st International Ciprofloxacin Workshop, Leverkusen, Nov. 6–8, 1985, pp. 157–159, Excerpta Medica, Amsterdam, 1986

    Google Scholar 

  • Schmidt W, Eigel P, Zürcher J, Dexling B, Sörgel F. Efficiency of ciprofloxacin prophylaxis in open-heart surgery: examination of its distribution into serum, myocardium, skeletal muscle and mediastinal fat. 2nd International Symposium on New Quinolones, Geneva, August 25–27, 1988. Abstract no. 72, 1988

  • Schramm P. Ofloxacin: concentration in human ejaculate and influence on sperm motility. Infection 14 (Suppl. 4): 274–275, 1986

    Article  Google Scholar 

  • Silvain C, Breux JP, Rochard E, Bouquet S, Becq-Giraudon B, et al. Decreased erythrocyte penetration of pefloxacin in cirrhotic patients. Journal of Antimicrobial Chemotherapy 20: 290–292, 1987

    Article  PubMed  CAS  Google Scholar 

  • Sörgel F, Jaehde U, Naber K, Schunack W. Pharmakokinetik und Analytik von Gyrase-Hemmern. 3. Einfluss der Lipophilie auf die Pharmakokinetik. In Naber et al. (Eds) Gyrase-Hemmer II. FAC 6-10, pp. 1987–1997, Futuramed Verlag, München, 1987a

    Google Scholar 

  • Sörgel F, Naber KG, Stephan U. Pharmakokinetik und Analytik von Gyrase-Hemmern. 1. Pharmakokinetik — ein Überblick. In Naber et al. (Eds) Gyrase-Hemmer II. FAC 6-10, pp. 1907–1961, Furturamed Verlag, München, 1987b

    Google Scholar 

  • Sörgel F, Mahr G, Koch HU, Stephan U, Wiesemann HG, et al. Effects of cimetidine on the pharmacokinetics of pefloxacin in healthy volunteers. Reviews of Infectious Diseases 10 (Suppl. 1): S137, 1988a

    Google Scholar 

  • Sörgel F, Mahr G, Stephan U, Koch HU, Wiesemann HG. Effect of normal and fat-rich food on the absorption of pefloxacin in humans. Reviews of Infectious Diseases 10 (Suppl. 1): S137–S138, 1988b

    Google Scholar 

  • Sörgel F, Mahr G, Stephan U, Koch HU, Wiesemann HG. Absolute bioavailability and pharmacokinetics of pefloxacin in healthy volunteers. Reviews of Infectious Diseases 10 (Suppl. 1): S93, 1988c

    Google Scholar 

  • Sörgel F, Koch HU, Malter U, Metz R, Mahr G, et al. Metabolism of pefloxacin in humans. Reviews of Infectious Diseases 10 (Suppl. 1): S95–S96, 1988d

    Google Scholar 

  • Sörgel F, Metz R, Naber K, Seelmann R, Muth P. Pharmacokinetics of fleroxacin in man. 1. Pharmacokinetics and body fluid penetration of fleroxacin in healthy volunteers. Journal of Antimicrobial Chemotherapy 22 (Suppl. D): 155–167, 1988e

    PubMed  Google Scholar 

  • Sörgel F, Seelmann R, Naber K, Metz R, Muth P. Pharmacokinetics of fleroxacin in man. 2. Metabolism of fleroxacin in man. Journal of Antimicrobial Chemotherapy 22 (Suppl. D): 169–178, 1988f

    PubMed  Google Scholar 

  • Sörgel F, Jaehde U, Zürcher J, Seelmann R, Muth P, et al. Effect of multiple dosing on nonrenal elimination of quinolones. 28th Interscience Conference of Antimicrobial Agents and Chemotherapy, October 23–26, Los Angeles, 1988. Abstract no. 1443, 1988g

  • Stahl JP, Croize J, Lefebvre MA, Bru JP, Guyot A, et al. Diffusion of ofloxacin into the cerebrospinal fluid in patients with bacterial meningitis. Infection 14 (Suppl. 4): 254–255, 1986

    Article  Google Scholar 

  • Stille W, Harder S, Mieke S, Beer C, Shah PM, et al. Decrease of caffeine elimination in man during co-administration of 4-quinolones. Journal of Antimicrobial Chemotherapy 20: 729–734, 1987

    Article  PubMed  CAS  Google Scholar 

  • Stübner G, Weinrich W, Brands U. Study of the cerebrospinal fluid penetrability of ofloxacin. Infections 14 (Suppl. 4): 250–253, 1986

    Article  Google Scholar 

  • Sullivan LP. Physiology of the kidney, p. 37, Lea & Febiger, Philadelphia, 1974

    Google Scholar 

  • Thys JP, Klastersky J, Jacobs F, Berre J, Gangji D, et al. Penetration of ciprofloxacin into bronchial secretions and pleural fluid. In Neu & Weuta (Eds) Proceedings of the 1st International Ciprofloxacin Workshop, Leverkusen. Nov. 6–8, 1985, pp. 153–156, Excerpta Medica, Amsterdam, 1986

    Google Scholar 

  • Uematsu M, Morihana T, Sekiguchi T, Imoto T, Sasaki J. The pharmacokinetics and saliva penetration of ofloxacin, norfloxacin, enoxacin and pipemidic acid. Proceedings of the 14th International Congress of Chemotherapy, Kyoto, 1985, pp. 1891–1892, 1985

  • Ullmann U, Giebel W, Dalhoff A, Koeppe P. Single and multiple dose pharmacokinetics of ciprofloxacin. European Journal of Clinical Microbiology 5: 193–196, 1986

    Article  PubMed  CAS  Google Scholar 

  • Unertl K, Dieterich HJ, Ruckdeschel G, Martin E, Ehret W. Lung tissue and serum concentrations of ciprofloxacin in patients. 15th International Congress of Chemotherapy, Istanbul, July 19–24, 1987. Abstract no. 1195, p. 324, 1987

  • Valainis G, Thomas D, Pankey G. Penetration of ciprofloxacin into cerebrospinal fluid. European Journal of Clinical Microbiology 5: 75–76, 1986

    Article  Google Scholar 

  • Weidekamm E, Portmann R, Suter K, Partos C, Dell D, et al. Single- and multiple-dose pharmacokinetics of fleroxacin, a trifluorinated quinolone, in humans. Antimicrobial Agents and Chemotherapy 31: 1909–1914, 1987

    Article  PubMed  CAS  Google Scholar 

  • Wijnands WJA, Vree TB, Van Herwaerden CLA. Enoxacin decreases the clearance of theophylline in man. British Journal of Clinical Pharmacology 20: 583–588, 1985

    Article  PubMed  CAS  Google Scholar 

  • Wijnands WJA, Vree TB, Baars AM, van Herwaarden CLA. Pharmacokinetics of enoxacin and its penetration into bronchial secretions and lung tissue. Journal of Antimicrobial Chemotherapy 21 (Suppl. B): 67–77, 1988

    Article  PubMed  CAS  Google Scholar 

  • Wingender W, Beermann D, Föerster D, Graefe KH, Schacht P, et al. Mechanism of renal excretion of ciprofloxacin (Bay o 9867), a new quinolone carboxylic acid derivative, in humans. Proceedings of the 4th Mediterranean Congress of Chemotherapy, Rhodos, 1984. Chemoterapia 4 (Suppl.): 403–404, 1985

    Google Scholar 

  • Wise R. The clinical relevance of protein binding and tissue concentrations in antimicrobial therapy. Clinical Pharmacokinetics 11: 470–482, 1986

    Article  PubMed  CAS  Google Scholar 

  • Wise R, Gillett AP, Cadge B, Durham SR, Baker S. The influence of protein binding upon tissue fluid levels of six β-lactam antibiotics. Journal of Infectious Diseases 142: 77–82, 1980

    Article  PubMed  CAS  Google Scholar 

  • Wise R, Lister D, McNulty CAM, Griggs D, Andrews JM. The comparative pharmacokinetics of five quinolones. Journal of Antimicrobial Chemotherapy 8 (Suppl. D): 71–81, 1986

    Google Scholar 

  • Wise R, Kirkpatrick B, Ashby J, Griggs DJ. Pharmacokinetics and tissue penetration of Ro 23-6240, a new trifluoroquinolone. 15th International Congress of Chemotherapy, Istanbul, July 19–24, 1987. Workshop on fleroxacin (Ro 23-6240): a new oral once-a-day quinolone. Abstract, p. 15, 1987

  • Wittmann DH, Kotthaus E. Further methodological improvement in antibiotic bone concentrations measurements: penetration of ofloxacin into bone and cartilage. Infection 14 (Suppl. 4): 270–273, 1986

    Article  Google Scholar 

  • Wolff M, Regnier B, Daldoss C, Nkam M, Vachon F. Penetration of pefloxacin into cerebrospinal fluid of patients with meningitis. Antimicrobial Agents and Chemotherapy 26: 289–291, 1984

    Article  PubMed  CAS  Google Scholar 

  • Woo FL, Johnson AP, Imsler MS, George WJ, La Corte WS. Gentamicin, tobramycin, amikacin and netilmicin levels in tears following intravenous administration. Archives of Ophthalmology 103: 216–218, 1985

    Article  PubMed  CAS  Google Scholar 

  • Zürcher J, Jaehde U, Sörgel F, Naber K, Schumacher H, et al. Distribution of enoxacin and its main metabolite oxo-enoxacin into saliva, nasal secretions, tears and sweat of healthy volunteers. 2nd International Symposium on New Quinolones, August 25–27, Geneva, 1988. Abstract no. 146, 1988a

  • Zürcher J, Jaehde U, Gottschalk B, Sörgel F, Naber K, et al. Effect of dose on bioavailability, pharmacokinetics and metabolism of pefloxacin following single and multiple dose administration. 2nd International Symposium on New Quinolones, August 25–27, Geneva, 1988. Abstract no. 69, 1988b

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Authors and Affiliations

  1. IBMP - Institute for Biomedical and Pharmaceutical Research, Harrichstrasse 5, D-8500, Nürnberg 10, Federal Republic of Germany

    Fritz Sörgel & Ulrich Jaehde

  2. Department of Urology, Elisabeth-Hospital, Straubing, Federal Republic of Germany

    Kurt Naber

  3. Department of Pediatrics, University of Essen, Essen, Federal Republic of Germany

    Ulrich Stephan

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  1. Fritz Sörgel
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  2. Ulrich Jaehde
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  3. Kurt Naber
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  4. Ulrich Stephan
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Sörgel, F., Jaehde, U., Naber, K. et al. Pharmacokinetic Disposition of Quinolones in Human Body Fluids and Tissues. Clin-Pharmacokinet 16 (Suppl 1), 5–24 (1989). https://doi.org/10.2165/00003088-198900161-00004

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  • DOI: https://doi.org/10.2165/00003088-198900161-00004

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