Comparative in vitro and bactericidal activity of oxazolidinone antibiotics against multidrug-resistant enterococci. 1998

G D Bostic, and M B Perri, and L A Thal, and M J Zervos
Department of Medicine, William Beaumont Hospital, Royal Oak, Michigan 48073, USA.

Increasing resistance among enterococci poses a considerable therapeutic problem. In this study, we evaluated the comparative in vitro activity of two investigational oxazolidinone antibiotics, eperezolid and linezolid, versus clinical isolates of multidrug-resistant enterococci. One hundred isolates (16 Enterococcus faecalis, 69 E. faecium, 10 E. gallinarum, 2 E. casseliflavus, 1 E. avium, 1 E. hirae, and 1 E. raffinosus) evaluated were collected from diverse geographic areas in North America and Europe from 1991 to 1995. Eperezolid MIC50 and MIC90 were 1.0 microgram/mL and 2.0 micrograms/mL (1.0-2.0 micrograms/mL range). Linezolid MIC50 and MIC90 were 2.0 micrograms/mL and 2.0 micrograms/mL (0.5-2.0 micrograms/mL range), respectively. MICs were the same at 10(3) CFU/mL and 10(8) CFU/mL initial inoculum. In time-kill experiments using 10 strains and concentrations of 4 micrograms/mL, 8 micrograms/mL, and 16 micrograms/mL (achievable serum concentrations) of eperezolid and linezolid there was a 2 log10 reduction of growth for 2 of 10 isolates tested using eperezolid and a 1 log10 reduction for 50% of isolates with both agents. There was indifferent bactericidal killing when either oxazolidinone was combined with gentamicin, ampicillin, or streptomycin for isolates lacking these resistances. This study demonstrates these oxazolidinone agents to have excellent in vitro activity versus multidrug-resistant enterococci.

UI MeSH Term Description Entries
D008826 Microbial Sensitivity Tests Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses). Bacterial Sensitivity Tests,Drug Sensitivity Assay, Microbial,Minimum Inhibitory Concentration,Antibacterial Susceptibility Breakpoint Determination,Antibiogram,Antimicrobial Susceptibility Breakpoint Determination,Bacterial Sensitivity Test,Breakpoint Determination, Antibacterial Susceptibility,Breakpoint Determination, Antimicrobial Susceptibility,Fungal Drug Sensitivity Tests,Fungus Drug Sensitivity Tests,Sensitivity Test, Bacterial,Sensitivity Tests, Bacterial,Test, Bacterial Sensitivity,Tests, Bacterial Sensitivity,Viral Drug Sensitivity Tests,Virus Drug Sensitivity Tests,Antibiograms,Concentration, Minimum Inhibitory,Concentrations, Minimum Inhibitory,Inhibitory Concentration, Minimum,Inhibitory Concentrations, Minimum,Microbial Sensitivity Test,Minimum Inhibitory Concentrations,Sensitivity Test, Microbial,Sensitivity Tests, Microbial,Test, Microbial Sensitivity,Tests, Microbial Sensitivity
D004352 Drug Resistance, Microbial The ability of microorganisms, especially bacteria, to resist or to become tolerant to chemotherapeutic agents, antimicrobial agents, or antibiotics. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS). Antibiotic Resistance,Antibiotic Resistance, Microbial,Antimicrobial Resistance, Drug,Antimicrobial Drug Resistance,Antimicrobial Drug Resistances,Antimicrobial Resistances, Drug,Drug Antimicrobial Resistance,Drug Antimicrobial Resistances,Drug Resistances, Microbial,Resistance, Antibiotic,Resistance, Drug Antimicrobial,Resistances, Drug Antimicrobial
D004359 Drug Therapy, Combination Therapy with two or more separate preparations given for a combined effect. Combination Chemotherapy,Polychemotherapy,Chemotherapy, Combination,Combination Drug Therapy,Drug Polytherapy,Therapy, Combination Drug,Chemotherapies, Combination,Combination Chemotherapies,Combination Drug Therapies,Drug Polytherapies,Drug Therapies, Combination,Polychemotherapies,Polytherapies, Drug,Polytherapy, Drug,Therapies, Combination Drug
D005839 Gentamicins A complex of closely related aminoglycosides obtained from MICROMONOSPORA purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit PROTEIN BIOSYNTHESIS. Gentamicin Sulfate (USP),Gentamycin,G-Myticin,Garamycin,Gentacycol,Gentamicin,Gentamicin Sulfate,Gentamycins,Gentavet,Genticin,G Myticin,GMyticin,Sulfate, Gentamicin
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000667 Ampicillin Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic. Penicillin, Aminobenzyl,Amcill,Aminobenzylpenicillin,Ampicillin Sodium,Ampicillin Trihydrate,Antibiotic KS-R1,Omnipen,Pentrexyl,Polycillin,Ukapen,Aminobenzyl Penicillin,Antibiotic KS R1,KS-R1, Antibiotic,Sodium, Ampicillin,Trihydrate, Ampicillin
D000900 Anti-Bacterial Agents Substances that inhibit the growth or reproduction of BACTERIA. Anti-Bacterial Agent,Anti-Bacterial Compound,Anti-Mycobacterial Agent,Antibacterial Agent,Antibiotics,Antimycobacterial Agent,Bacteriocidal Agent,Bacteriocide,Anti-Bacterial Compounds,Anti-Mycobacterial Agents,Antibacterial Agents,Antibiotic,Antimycobacterial Agents,Bacteriocidal Agents,Bacteriocides,Agent, Anti-Bacterial,Agent, Anti-Mycobacterial,Agent, Antibacterial,Agent, Antimycobacterial,Agent, Bacteriocidal,Agents, Anti-Bacterial,Agents, Anti-Mycobacterial,Agents, Antibacterial,Agents, Antimycobacterial,Agents, Bacteriocidal,Anti Bacterial Agent,Anti Bacterial Agents,Anti Bacterial Compound,Anti Bacterial Compounds,Anti Mycobacterial Agent,Anti Mycobacterial Agents,Compound, Anti-Bacterial,Compounds, Anti-Bacterial
D013293 Enterococcus faecalis A species of gram-positive, coccoid bacteria commonly isolated from clinical specimens and the human intestinal tract. Most strains are nonhemolytic. Streptococcus Group D,Streptococcus faecalis
D013307 Streptomycin An antibiotic produced by the soil actinomycete Streptomyces griseus. It acts by inhibiting the initiation and elongation processes during protein synthesis. Estreptomicina CEPA,Estreptomicina Clariana,Estreptomicina Normon,Strepto-Fatol,Strepto-Hefa,Streptomycin GrĂ¼nenthal,Streptomycin Sulfate,Streptomycin Sulfate (2:3) Salt,Streptomycin Sulphate,Streptomycine Panpharma,Strepto Fatol,Strepto Hefa
D016984 Enterococcus faecium A species of gram-positive, coccoid bacteria whose organisms are normal flora of the intestinal tract. Unlike ENTEROCOCCUS FAECALIS, this species may produce an alpha-hemolytic reaction on blood agar and is unable to utilize pyruvic acid as an energy source. Streptococcus faecium

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