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Microbiological and pharmacokinetic evaluation of cefonicid, a long-acting cephalosporin
Abstract:
The in vitro antimicrobial activity of cefonicid has been tested against 27 recent clinical isolates of 7 different species (S. aureus, E. coli, K. pneumoniae, P. mirabilis, S. marcescens, E. cloacae and P. aeruginosa) using the MS-2 Research System, contrast phase microscopy and the colony forming unit assay. With the exception of P. aeruginosa, S. marcescens and E. cloacae, cefonicid showed excellent activity against the different bacterial species tested (i.e. S. aureus, E. coli, K. pneumoniae and P. mirabilis). Tissue penetration of cefonicid after a single i.m. or i.v. dose (1 or 2 g, respectively) was also studied using the suction blister method. In 14 adult subjects with normal renal and liver functions, cefonicid plasma half-life was 5.1 and 5.4 h following i.v. and i.m. administration. Drug concentrations achieved at peak in plasma and suction blister fluid were higher than the minimum inhibitory concentrations for most sensitive pathogens and remained above these values for 24 h. These data support the use of a single daily dose regimen of cefonicid, both i.v. and i.m., for the treatment of most common infections caused by sensitive pathogens in blood and tissues.
Insights
Cefonicid demonstrates potent in vitro antimicrobial activity against common bacterial pathogens like S. aureus and E. coli. Tissue penetration and sustained plasma concentrations support a single daily dose for treating infections.
Area of Science:
- Pharmacology
- Microbiology
- Infectious Diseases
Background:
- Cefonicid is a cephalosporin antibiotic.
- Understanding its efficacy and pharmacokinetic profile is crucial for clinical application.
Purpose of the Study:
- To evaluate the in vitro antimicrobial activity of cefonicid against clinical bacterial isolates.
- To assess cefonicid's tissue penetration and pharmacokinetic properties in humans.
Main Methods:
- In vitro testing using MS-2 Research System, microscopy, and CFU assays.
- Suction blister method for tissue penetration studies.
- Pharmacokinetic analysis of plasma and blister fluid concentrations.
Main Results:
- Cefonicid exhibited excellent activity against S. aureus, E. coli, K. pneumoniae, and P. mirabilis.
- Plasma half-life was approximately 5.1-5.4 hours.
- Achieved therapeutic concentrations in plasma and blister fluid, sustained for 24 hours.
Conclusions:
- Cefonicid shows significant antimicrobial activity against key pathogens.
- Favorable pharmacokinetics support a once-daily dosing regimen.
- Supports cefonicid's use for treating common bacterial infections in blood and tissues.