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Pharmacokinetics of the quinolones in volunteers : a proposed dosing schedule

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Wise, R., Griggs, Deborah and Andrews, J. M. (1988) Pharmacokinetics of the quinolones in volunteers : a proposed dosing schedule. Reviews of infectious diseases, Vol.10 (Suppl 1). S83-S89. doi:10.1093/clinids/10.Supplement_1.S83 ISSN 0162-0886.

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Official URL: http://www.jstor.org/stable/4454354

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Abstract

The pharmacokinetics and tissue penetration of five quinolones into inflammatory exudate were studied in healthy volunteers. The compounds studied were norfloxacin (400 mg orally), enoxacin (400 mg intravenously and 600 mg orally), ciprofloxacin (100 mg intravenously and 500 mg orally), ofloxacin (600 mg orally), and pefloxacin (400 mg intravenous). Orally administered ofloxacin and ciprofloxacin were the most rapidly absorbed (time to maximal serum level, 1.2 hours) and enoxacin the least (1.9 hours). The serum levels attained were highest in the case of ofloxacin (after an allowance was made for the higher dose administered). The serum elimination half-lives were as follows: norfloxacin, 3.75 hours; ciprofloxacin, 3.9 hours (oral) and 4.0 hours (intravenous); ofloxacin, 7.0 hours; enoxacin, 6.2 hours (oral) and 5.1 hours (intravenous); and pefloxacin, 10.5 hours. All agents penetrated well into a mild inflammatory exudate. The 24-hour recovery rate from urine was 62% for oral enoxacin, 46.4% for intravenous enoxacin (plus 12.2% for oxo-enoxacin), 27% for norfloxacin, 30.6% for oral ciprofloxacin, 75.7% for intravenous ciprofloxacin, 73% for ofloxacin, and 4.9% for pefloxacin (plus 9.2% for the norfloxacin metabolite and 17.8% for pefloxacin N-oxide). A dosing schedule for the quinolones was proposed on the basis of pharmacokinetic parameters and microbiologic activity.

Item Type: Journal Article
Divisions: Faculty of Science, Engineering and Medicine > Medicine > Warwick Medical School
Journal or Publication Title: Reviews of infectious diseases
Publisher: Oxford University Press
ISSN: 0162-0886
Official Date: 1988
Dates:
DateEvent
1988Published
Volume: Vol.10
Number: Suppl 1
Page Range: S83-S89
DOI: 10.1093/clinids/10.Supplement_1.S83
Status: Peer Reviewed
Publication Status: Published

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