The pharmacokinetics and serum and urine bactericidal activity of ciprofloxacin.
Ciprofloxacin is an investigational quinolone agent possessing an impressive antibacterial spectrum. Its pharmacokinetics were studied in six volunteers after 250-mg and 500-mg single oral doses, and its bactericidal activity compared to that of trimethoprim-sulfamethoxazole given to the same volunteers. Mean peak serum levels were 1.45 micrograms/mL and 2.46 micrograms/mL for 250-mg and 500-mg doses, and time to peak was 1 and 1.3 hours. The 12-hour levels were 0.12 micrograms and 0.22 microgram. Half-life (T1/2)alpha were 0.32 and 0.43 with T1/2 beta were 3.97 and 4.15 and volume of distribution (area) were 80L and 90L, respectively. Area under the concentration curve (AUC) was 5.65 h X micrograms/mL and 10.37h X micrograms/mL. Serum clearance was 23L for both doses. Approximately 49% of the 250-mg dose and 43% of the 500-mg dose was recovered in the urine. Bactericidal levels were determined against clinical isolates. Sera at 1.5 hours after the 500-mg dose averaged bactericidal levels of 1:20 or better for an Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and beta-lactamase producing Haemophilus influenzae and Branhamella catarrhalis. Urinary bactericidal levels at eight to 12 hours were greater than or equal to 1:157 for E coli, K pneumoniae, gentamicin-piperacillin resistant P aeruginosa, Staphylococcus aureus, and 1:20 for Streptococcus faecalis. Serum bactericidal levels were superior, and urine bactericidal levels were superior or equal to the bactericidal levels obtained with trimethoprim-sulfamethoxazole.(ABSTRACT TRUNCATED AT 250 WORDS)
Brittain
D C
DC
Scully
B E
BE
McElrath
M J
MJ
Steinman
R
R
Labthavikul
P
P
Neu
H C
HC
D000328:Adult; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000378:metabolism*; D000892:Anti-Infective Agents, Urinary / Q000008:administration & dosage / Q000378:metabolism*; D001437:Bacteriuria; D001770:Blood Bactericidal Activity; D002939:Ciprofloxacin; D002986:Clinical Trials as Topic; D004311:Double-Blind Method; D004338:Drug Combinations / Q000378:metabolism; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006801:Humans; D007700:Kinetics; D008297:Male; D011804:Quinolines / Q000008:administration & dosage / Q000378:metabolism* / Q000494:pharmacology; D011897:Random Allocation; D013419:Sulfamethizole / Q000378:metabolism; D013997:Time Factors; D014295:Trimethoprim / Q000378:metabolism; D000096926:Benzenesulfonamides
D000900:Anti-Bacterial Agents; D000892:Anti-Infective Agents, Urinary; D002939:Ciprofloxacin; D004338:Drug Combinations; D011804:Quinolines; D013419:Sulfamethizole; D014295:Trimethoprim; C029078:trimethoprim sulfamethizole; D000096926:Benzenesulfonamides