Plasma bactericidal activity of a new C-5 methyl fluoroquinolone after oral doses of 400 and 800 mg.

Abstract

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.

• Authors: J W Gu, W Fang, H C Neu
• Journal: Journal of clinical pharmacology (J Clin Pharmacol) Vol. 32 Issue 9 Pg. 804-7 (Sep 1992) ISSN: 0091-2700 [Print] England
• PMID: 1331205 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Anti-Infective Agents
• Fluoroquinolones
• Piperazines
• Quinolones
• grepafloxacin

Topics

• Administration, Oral
• Anti-Infective Agents (administration & dosage, blood, pharmacology)
• Bacteria (drug effects)
• Drug Administration Schedule
• Fluoroquinolones
• Humans
• Male
• Microbial Sensitivity Tests
• Piperazines (administration & dosage, blood, pharmacology)
• Quinolones (administration & dosage, blood, pharmacology)