The influence of protein binding on the antibacterial activity of faropenem against Haemophilus influenzae

Clinical Microbiology and Infection : the Official Publication of the European Society of Clinical Microbiology and Infectious Diseases
I Gustafsson, O Cars

Abstract

The effects of albumin and human serum on the pharmacodynamics of faropenem were studied. The protein binding of faropenem was 91-95%, corresponding to the increase in MICs for Haemophilus influenzae in broth supplemented with albumin. Time-kill experiments in albumin-containing medium and in inactivated human serum 50% v/v showed that much higher drug concentrations were needed to achieve a bactericidal effect than were needed in broth. Active human serum alone exerted a strain-dependent bactericidal effect. It was concluded that it is the free fraction of faropenem in serum that has antibacterial activity against H. influenzae.

References

Jan 1, 1997·Journal of Pharmaceutical Sciences·A KovarH Derendorf
Jan 1, 1997·The Journal of Antimicrobial Chemotherapy·J M WoodcockR Wise
Feb 10, 1998·Clinical Infectious Diseases : an Official Publication of the Infectious Diseases Society of America·W A Craig
Apr 30, 2002·International Journal of Antimicrobial Agents·Ping LiuHartmut Derendorf
Oct 3, 2002·The Journal of Antimicrobial Chemotherapy·F J BoswellR Wise

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Citations

May 4, 2011·Antimicrobial Agents and Chemotherapy·Markus A ZeitlingerUrsula Theuretzbacher
Dec 21, 2007·The Annals of Pharmacotherapy·Jacob P GettigAlexander H Philbrick
Nov 22, 2017·Antimicrobial Agents and Chemotherapy·Axel Dalhoff
Apr 5, 2013·Clinical Microbiology Reviews·Daniel GonzalezHartmut Derendorf

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