Linezolid (Zyvox), the first of a new class of antibiotics, the oxazolidinones, is approved for treatment of Gram-positive bacterial infections, including resistant strains. The disposition of linezolid in human volunteers was determined, after a 500-mg (100-mCi) oral dose of [C]linezolid. Radioactive linezolid was administered as a single dose, or at steady-state on day 4 of a 10-day, 500-mg b...

Introduction In the past years, several studies have reported about the use of linezolid in the treatment of orthopaedic bone and joint infections, especially those caused by multiresistant bacteria. However, inhomogeneities in the patients’ collectives, primary surgical indication, causative pathogenic organisms, length of therapy and length of follow-up make a sufficient comparison of these s...

Oritavancin (MIC50/90, 0.03/0.06 to 0.12 μg/ml) had potent activity against linezolid-resistant staphylococci, as well as Enterococcus faecalis and Enterococcus faecium (oritavancin MIC50/90, 0.015/0.12 μg/ml against both species). All linezolid-resistant isolates were inhibited by oritavancin at ≤0.12 μg/ml. These results confirmed the absence of cross-resistance between linezolid and oritavan...

There is an urgent need for better regimens to treat drug-resistant tuberculosis (DR-TB). Treatment for multi-drug resistant tuberculosis (MDR-TB, defined as resistance to both isoniazid and rifampicin) has a success rate of only 64% (Falzon et al., 2013), is prolonged for up to 24 months, and is poorly tolerated. Treatment success for extensively drug-resistant tuberculosis (XDR-TB, defined as...

Eperezolid and linezolid are representatives of a new class of orally active, synthetic antimicrobial agents. The in vitro activity values (MICs) of linezolid, eperezolid, and comparator antibiotics against 102 strains of Rhodococcus equi isolated from humans and animals were determined. Linezolid was more active than eperezolid against the strains tested; premafloxacin was the most active comp...

The intracellular penetration and activity of linezolid in human polymorphonuclear leukocytes and tissue-cultured cells (McCoy) were evaluated. Linezolid reached intracellular concentrations slightly greater than extracellular ones in both types of cell. The uptake was rapid and not saturable and was affected by environmental temperature and cell viability. Linezolid showed slight intracellular...

Linezolid, the first oxazolidinone class agent to be introduced clinically, has broad activity against many important multidrug-resistant Gram-positive pathogens, including methicillinresistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). Linezolid inhibits protein synthesis by interacting with 23S rRNA in the 50S ribosomal subunit, and it should interfere with the b...

Sir, Linezolid, a new oxazolidinone, has a unique mode of action.1 The antimicrobial agent has a wide spectrum of activity against Gram-positive organisms, including methicillinresistant Staphylococcus aureus,2,3 penicillin-resistant pnemococci3 and both vancomycin-resistant Enterococcus faecalis and Enterococcus faecium.3,4 Linezolid is available in oral and intravenous (iv) preparations and n...

Use of combinations of antimicrobials that together achieve synergistic activities against targeted microorganisms is one potential strategy for overcoming bacterial resistance. As the incidence of infections caused by multidrug-resistant staphylococci and enterococci increases, the importance of devising additional synergistic drug combinations for these bacteria is magnified. We evaluated a n...

OBJECTIVES To characterize linezolid resistance among blood cultured Staphylococcus epidermidis from patients at the Polyclinic Agostino Gemelli (2006-08). Isolates also showed elevated MICs of macrolide, lincosamide and streptogramin (MLS) compounds, which were investigated. METHODS Ten S. epidermidis exhibiting linezolid MICs ≥ 4 mg/L were included. Isolates were screened for cfr mutations ...