title: The influence of protein binding on the antibacterial activity of faropenem against Haemophilus influenzae.
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.
authors.affiliation: Antibiotic Research Unit, Department of Medical Sciences, Clinical Bacteriology and Infectious Diseases, Uppsala University, Uppsala, Sweden.
authors.forename: I
authors.initials: I
authors.lastname: Gustafsson
authors.forename: O
authors.initials: O
authors.lastname: Cars
mesh_terms: D015780:Carbapenems / Q000494:pharmacology*; D015169:Colony Count, Microbial; D006192:Haemophilus Infections / Q000382:microbiology; D006193:Haemophilus influenzae / Q000187:drug effects* / Q000302:isolation & purification / Q000378:metabolism*; D006801:Humans; D007769:Lactams / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D011485:Protein Binding; D012709:Serum Albumin / Q000378:metabolism* / Q000494:pharmacology; D015610:Serum Bactericidal Test; D001618:beta-Lactamases / Q000378:metabolism; D047090:beta-Lactams
chemical_list: D015780:Carbapenems; D007769:Lactams; D012709:Serum Albumin; D047090:beta-Lactams; D001618:beta-Lactamases; C107057:fropenem