, Volume 14, Supplement 3, pp S196–S202 | Cite as

The comparative pharmacokinetics and tissue penetration of four quinolones including intravenously administered enoxacin

  • R. Wise
  • D. Lister
  • C. A. M. McNulty
  • D. Griggs
  • J. M. Andrews


The pharmacokinetics and tissue penetration of four quinolones were studied. The compounds were norfloxacin (400 mg p.o.), enoxacin (600 mg p.o. and 400 mg i.v.), ciprofloxacin (100 mg i.v. and 500 mg p.o.) and ofloxacin (600 mg p.o.) given to healthy volunteers. Of the oral agents studied ofloxacin and ciprofloxacin were the most rapidly absorbed (Tmax 1.2 h) and enoxacin the least (Tmax 1.9 h). The serum levels attained were highest in the case of ofloxacin (after allowing for the higher dose administered). The serum half-lives were norfloxacin 3.75 h, ciprofloxacin 3.9 h (p.o.), 4.0 h (i.v.), ofloxacin 7.0 h and enoxacin 6.2 h (p.o.) and 5.1 h (i.v.). All agents penetrated the blister fluid readily. The 24 h urine recovery (as measured by a microbiological assay) was 62% for enoxacin (p.o.), 46.4% following i.v. enoxacin (plus 11.6% oxo-enoxacin, measured by HPLC) 27% for norfloxacin, 30.6% for oral ciprofloxacin, 75.7% for i.v. ciprofloxacin and 73% for ofloxacin.


HPLC Healthy Volunteer General Practice Family Medicine Ofloxacin 
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Vergleichende Pharmakokinetik und Gewebepenetration von vier Chinolonen einschließlich intravenös appliziertem Enoxacin


Die Pharmakokinetik und Gewebepenetration von vier Chinolonen wurde bestimmt. Die untersuchten Verbindungen waren Norfloxacin (400 mg p.o.), Enoxacin (600 mg p.o. und 400 mg i.v.), Ciprofloxacin (100 mg i.v. und 500 mg p.o.) sowie Ofloxacin (600 mg p.o.). Die Untersuchungen wurden an gesunden freiwilligen Probanden durchgeführt. Von den untersuchten oralen Substanzen wurden Ofloxacin und Ciprofloxacin am schnellsten resorbiert (Tmax 1,2 Stunden) und Enoxacin am langsamsten (Tmax 1,9 Stunden). Ofloxacin erreichte die höchsten Serumspiegel (nach Gabe der höheren Dosis). Die Serumhalbwertszeiten betrugen für Norfloxacin 3,75 Stunden, für Ciprofloxacin 3,9 Stunden (p.o.), 4,0 Stunden (i.v.), für Ofloxacin 7,0 Stunden und für Enoxacin 6,2 Stunden (p.o.) und 5,1 Stunden (i.v.). Alle Substanzen penetrierten rasch in Hautblasenflüssigkeit. Die Wiederfindungsrate im 24-Stunden-Urin (gemessen mittels mikrobiologischem Assay) betrug für Enoxacin 62% (p.o.), 46,1% nach i.v.-Gabe (plus 11,6% Oxoenoxacin, bestimmt mittels HPLC) und für Norfloxacin 27%, für orales Ciprofloxacin 30,6%, für i.v. appliziertes Ciprofloxacin 75,7%, sowie für Ofloxacin 73%.


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Copyright information

© MMV Medizin Verlag GmbH München 1986

Authors and Affiliations

  • R. Wise
    • 1
  • D. Lister
    • 1
  • C. A. M. McNulty
    • 1
  • D. Griggs
    • 1
  • J. M. Andrews
    • 1
  1. 1.Microbiology DepartmentDudley Road HospitalBirminghamEngland

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