Effect of ertapenem protein binding on killing of bacteria.
The effect of protein binding on the antimicrobial activity of ertapenem was evaluated using the bacterial kill rate and concentration-response studies. Various proportions of human serum were utilized to determine the total and free-drug concentrations using a validated high-performance liquid chromatography assay. The MICs and kill curves were determined for test isolates of Enterobacter cloacae and Staphylococcus aureus at various percentages of human serum. The killing of bacteria was analyzed in relation to the free and total concentrations of ertapenem at various proportions of human serum. It was determined that unbound ertapenem was responsible for the antimicrobial activity against the test isolates.
Nix
David E
DE
Department of Pharmacy Practice and Science, College of Pharmacy, University of Arizona, 1703 E. Mabel St., P.O. Box 210-207, Tucson, AZ 85721-0207, USA. nix@pharmacy.arizona.edu
Matthias
Kathryn R
KR
Ferguson
Emily C
EC
D001419:Bacteria / Q000187:drug effects*; D002851:Chromatography, High Pressure Liquid; D016972:Enterobacter cloacae / Q000187:drug effects; D004756:Enterobacteriaceae Infections / Q000382:microbiology; D000077727:Ertapenem; D006801:Humans; D007202:Indicators and Reagents; D007700:Kinetics; D007769:Lactams / Q000378:metabolism* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D011485:Protein Binding; D012044:Regression Analysis; D013056:Spectrophotometry, Ultraviolet; D013203:Staphylococcal Infections / Q000382:microbiology; D013211:Staphylococcus aureus / Q000187:drug effects; D047090:beta-Lactams
D007202:Indicators and Reagents; D007769:Lactams; D047090:beta-Lactams; D000077727:Ertapenem