Plasma bactericidal activity of a new C-5 methyl fluoroquinolone after oral doses of 400 and 800 mg.
The plasma bactericidal activity of a new C-5 methyl fluoroquinolone, OPC-17116, was determined after once-daily oral ingestion of 400 mg and 800 mg in normal, healthy volunteers. OPC-17116 at a 400-mg dose produced plasma bactericidal titers greater than or equal to 1:16 at 12 hours against Escherichia coli, Klebsiella pneumoniae, Serratia marcescens, Haemophilus influenzae, and Moraxella catarrhalis. OPC-17116 bactericidal titers against Pseudomonas aeruginosa were 1:2 or 1:4 at 6 and 12 hours. The plasma bactericidal titers against Streptococcus pyogenes and Streptococcus pneumoniae were 1:4 or greater, but bactericidal titers against Staphylococcus aureus were 1:2 at 12 hours and less than 1:2 at 24 hours. The 800-mg dose of OPC-17116 produced bactericidal titers of at least 1:32 at 12 hours for the Enterobacteriaceae, Haemophilus, and Moraxella, and 1:4 for S. pyogenes and S. pneumoniae, but bactericidal titers against S. aureus were 1:2. These data would suggest that an 800-mg dose of OPC-17116 taken orally once daily would provide adequate concentrations to treat infections due to the pathogens examined in this study.
Gu
J W
JW
Department of Medicine, College of Physicians and Surgeons, Columbia University, New York, New York.
Fang
W
W
Neu
H C
HC
D000284:Administration, Oral; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000097:blood / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D004334:Drug Administration Schedule; D024841:Fluoroquinolones; D006801:Humans; D008297:Male; D008826:Microbial Sensitivity Tests; D010879:Piperazines / Q000008:administration & dosage / Q000097:blood / Q000494:pharmacology*; D015363:Quinolones / Q000008:administration & dosage / Q000097:blood / Q000494:pharmacology*
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D010879:Piperazines; D015363:Quinolones; C075375:grepafloxacin