Literature DB >> 15373892

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

I Gustafsson1, 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.

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Year:  2004        PMID: 15373892     DOI: 10.1111/j.1469-0691.2004.00977.x

Source DB:  PubMed          Journal:  Clin Microbiol Infect        ISSN: 1198-743X            Impact factor:   8.067


  5 in total

Review 1.  Protein binding of antimicrobials: methods for quantification and for investigation of its impact on bacterial killing.

Authors:  Jürgen Beer; Claudia Christina Wagner; Markus Zeitlinger
Journal:  AAPS J       Date:  2009-01-01       Impact factor: 4.009

Review 2.  Protein binding: do we ever learn?

Authors:  Markus A Zeitlinger; Hartmut Derendorf; Johan W Mouton; Otto Cars; William A Craig; David Andes; Ursula Theuretzbacher
Journal:  Antimicrob Agents Chemother       Date:  2011-05-02       Impact factor: 5.191

Review 3.  Importance of relating efficacy measures to unbound drug concentrations for anti-infective agents.

Authors:  Daniel Gonzalez; Stephan Schmidt; Hartmut Derendorf
Journal:  Clin Microbiol Rev       Date:  2013-04       Impact factor: 26.132

Review 4.  Seventy-Five Years of Research on Protein Binding.

Authors:  Axel Dalhoff
Journal:  Antimicrob Agents Chemother       Date:  2018-01-25       Impact factor: 5.191

5.  Posaconazole in human serum: a greater pharmacodynamic effect than predicted by the non-protein-bound serum concentration.

Authors:  Anders Lignell; Elisabeth Löwdin; Otto Cars; Erja Chryssanthou; Jan Sjölin
Journal:  Antimicrob Agents Chemother       Date:  2011-04-18       Impact factor: 5.191

  5 in total

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