Comparative pharmacokinetics and safety of ciprofloxacin 400 mg i.v. thrice daily versus 750 mg po twice daily

• Published in: Journal of antimicrobial chemotherapy Vol. 33; no. 4; p. 795
• Main Authors: Shah, A, Lettieri, J, Kaiser, L, Echols, R, Heller, A H
• Format: Journal Article
• Language: English
• Published: England 01-04-1994
• Subjects: Administration, Oral; Adult; Alanine Transaminase - blood; Aspartate Aminotransferases - blood; Ciprofloxacin - administration & dosage; Ciprofloxacin - adverse effects; Ciprofloxacin - pharmacokinetics; Double-Blind Method; Humans; Injections, Intravenous; Male
• ISSN: 0305-7453
• DOI: 10.1093/jac/33.4.795

Comparative pharmacokinetics of i.v. and oral ciprofloxacin was studied in 24 healthy male subjects given 400 mg i.v. tds or 750 mg po bd in a randomized, double-blind, placebo controlled, crossover fashion with at least a 10 day washout period. Blood and urine samples were obtained following the first (single dose) and last (steady state) dose in each treatment period. After single dosing and under steady state conditions, the calculated 24 h area under the serum concentration versus time curve, (AUC0-24) after 400 mg i.v. tds (AUC0-8 x 3) was equivalent to the AUC0-24 after 750 mg po bd (AUC0-12 x 2). Peak serum concentrations produced by the i.v. regimen were very similar to those observed after the 750 mg oral dose. The extent of accumulation was similar following either dosing regimen and was approximately 35%. Overall, the incidence of adverse effects (none of which was serious) was higher with the i.v. regimen than with the oral regimen, mainly due to injection site reaction, which was the most commonly reported adverse event.