JAC Advance Access published online on September 6, 2002
Journal of Antimicrobial Chemotherapy, doi:10.1093/jac/dkf155
© 2002 by The British Society for Antimicrobial Chemotherapy
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Original Paper
1 Department of Microbiology, City Hospital NHS Trust, Birmingham
B18 7QH, UK
* Corresponding author. E-mail: r.wise{at}bham.ac.uk.
Received 29 November 2001
; revised 5 June 2002
; accepted 21 June 2002
The influence of protein binding upon different aspects
of the in vitro activity of faropenem on recently
isolated Staphylococcus aureus and respiratory
pathogens was determined. The protein binding of faropenem was investigated
in inactivated human serum and albumin by ultrafiltration. The effect
of the presence of inactivated human serum and albumin on the in vitro activity of faropenem and amoxicillin
was established and the influence of protein binding on the pharmacodynamic
properties of faropenem and amoxicillin was compared. The protein
binding of faropenem was 96% and 95% in pooled
inactivated human serum and 99% and 98% in 45
mg/L human albumin, at 8 and 25 mg/L, respectively. The presence
of inactivated human serum (20% and 70%)
increased the mean faropenem MICs by two dilution steps and albumin
increased the mean faropenem MICs by three dilution steps. The mean
amoxicillin MICs were less affected than faropenem by the presence
of either inactivated human serum or albumin. Faropenem and amoxicillin
exhibited similar time-dependent kinetics. Faropenem was bacteriostatic
on Moraxella catarrhalis, Haemophilus
influenzae and group A streptococci, and bactericidal for Streptococcus pneumoniae (after 4 h with concentrations
equivalent to 5 x and 10 x MIC)
in Iso-Sensitest broth. In 70% inactivated human serum
faropenem was slowly bactericidal against M. catarrhalis, H. influenzae (one strain) and S. pneumoniae (one
strain) but not group A streptococci and the other S.
pneumoniae strain. A significant inoculum effect was observed
with all strains except S. pneumoniae. Both faropenem
and amoxicillin appeared more active in 70% inactivated
human serum than in Iso-Sensitest broth.
Effect of protein binding on the in
vitro activity and pharmacodynamics
of faropenem
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