title: Pharmacokinetics and safety of single rising doses of ofloxacin in healthy volunteers.
abstract: The pharmacokinetics, safety, and disposition of the new antimicrobial fluoroquinolone ofloxacin were evaluated after oral administration in 14 healthy, male volunteers in a double-blind, placebo-controlled study. Ofloxacin was administered as 100-, 300-, and 600-mg doses separated by 1 week. Plasma and urine concentrations after each administration were measured using a sensitive and specific high-performance liquid chromatographic procedure. The distribution of ofloxacin was modeled using a two-compartment open-body model with first-order absorption. Maximum plasma concentrations and area under the plasma concentration versus time curve increased in a linear, dose-proportional manner over the range studied. At all levels, within 36 hours after administration, approximately 70% of the dose was recovered in urine as unchanged ofloxacin and only minimal amounts (less than 4%) as metabolites. No significant changes in the distribution or elimination of the compound were found over the 6-fold dose range. No major laboratory toxicities or clinically significant adverse effects were noted in either the ofloxacin or placebo group.
authors.affiliation: Antiinfective Pharmacology Research Unit, University of Rhode Island College of Pharmacy, Providence.
authors.forename: C R
authors.initials: CR
authors.lastname: Marchbanks
authors.forename: M N
authors.initials: MN
authors.lastname: Dudley
authors.forename: S
authors.initials: S
authors.lastname: Flor
authors.forename: B
authors.initials: B
authors.lastname: Beals
mesh_terms: D000284:Administration, Oral; D000328:Adult; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D006801:Humans; D008297:Male; D015242:Ofloxacin / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine
chemical_list: D015242:Ofloxacin