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Excellent tissue penetration and 100% oral bioavailability are notable properties of linezolid (Zyvox).

Linezolid is active against nearly all antibiotic resistant gram-positive bacteria.

It is more effective than glycopeptides, macrolides and beta-lactams for skin and soft tissue infections.

Compared with other antibacterials, linezolid is associated with a greater frequency of side effects, mainly nausea, vomiting, diarrhea and headaches. Thrombocytopenia also occurs more frequently in patients taking linezolid but there is no increased frequency of anemia. Peripheral or optic neuropathy is associated with long duration of treatment (3-6 months).

Linezolid is very expensive compared to most other antibiotics.

• Skin and soft tissue infection
  Linezolid is superior to teicoplanin in the treatment of skin infections1.
• Pneumonia
  Linezolid is superior to teicoplanin in the treatment of pneumonia1.
• Bacteremia (presence of bacteria in the bloodstream)
  Linezolid is superior to teicoplanin in the treatment of Gram-positive bacteremia.
  In the randomized, controlled study1 linezolid demonstrated a 31.8% treatment advantage over teicoplanin in the treatment of Gram-positive bacteremia. The majority (9/13) of teicoplanin treatment failures were in S. aureus infections, and of these, almost all (8/9) were associated with methicillin-susceptible strains. Available MIC results did not indicate that teicoplanin resistance in vitro was an explanation for such treatment failure.

The possible reason for efficacy differences between teicoplanin and linezolid is superior pharmacokinetic properties of the latter.

Side effects

Linezolid produces higher rates of gastrointestinal side effects (nausea, vomiting, diarrhea).

• Pneumonia
  The available evidence suggests that linezolid is at least as effective as vancomycin for the treatment nosocomial pneumonia. There are some retrospective analyses supporting linezolid superiority in comparison with vancomycin for MRSA nosocomial pneumonia, including ventilator-associated pneumonia.
  Studies comparing vancomycin with linezolid in the treatment of Methicillin-resistant S. aureus (MRSA) pneumonia showed a significantly better survival rates with linezolid as compared to vancomycin3. Lung penetration advantages of linezolid over vancomycin are likely to be the reason.
• Skin and soft tissue infection
  Linezolid is equivalent to vancomycin in treating complicated skin and soft tissue infections and superior to vancomycin in the treatment of infections due to Methicillin-resistant S. aureus (MRSA)4,7.
  Better results with linezolid are related to the enhanced skin and tissue penetration of linezolid.

The high bioavailability (close to 100%) of linezolid translates to reduced length of hospital stay compared with vancomycin, which may offset its several-fold higher acquisition cost.

Linezolid may be particularly useful as an alternative to vancomycin in patients who have impaired renal function, poor or no intravenous access, require outpatient therapy, or who don't tolerate glycopeptides.

Skin and skin structure infections

Linezolid is as effective as cefadroxil in treating uncomplicated skin infections.

In a randomized, blinded, multicenter trial comparing linezolid to cefadroxil for the treatment of uncomplicated skin and soft tissue infections in children, clinical cure rates were not significantly different between two antibiotic treatments (91% for linezolid and 90% for cefadroxil)5. Both drugs were well tolerated, with a comparable rate of serious side effects (0.8% for linezolid and 1.6% for cefadroxil).

Diabetic foot infections

Linezolid is at least as effective as aminopenicillin/betalactamase inhibitors for the treatment of diabetic foot infections.

The open-label, randomized trial compared the efficacy and safety of linezolid versus ampicillin-sulbactam or amoxicillin-clavulanate in various types of diabetic foot infections6. Participants were randomized to receive linezolid or ampicillin-sulbactam or amoxicillin-clavulanate. The clinical cure (elimination of symptoms) rates were 81% for linezolid and 71% for the betalactam group. Side effects were more frequent with linezolid treatment, primarily diarrhea (8%), nausea (6%), anemia (5%), and thrombocytopenia (4%).

Skin and skin-structure infection

Oral linezolid was compared with oral clarithromycin in a multinational double-blind trial for patients with uncomplicated (not requiring adjunctive invasive therapy) skin and skin-structure infection2. In the clinically evaluable subset, linezolid-treated patients had a clinical response of 88%; in the clarithromycin group, the clinical response rate was 85%.

• Linezolid (Zyvox) Medical Facts

• 1. Wilcox M, Nathwani D, Dryden M. Linezolid compared with teicoplanin for the treatment of suspected or proven Gram-positive infections. Journal of Antimicrobial Chemotherapy. 2004 Feb;53(2):335-44.
• 2. Duvall SE, Seas C, Bruss JB, et al. Comparison of linezolid to oral clarithromycin in the treatment of uncomplicated skin infections: results from a multinational phase III trial. In: Program and abstracts of the 9th International Congress of Infectious Diseases; April 10-13, 2000;
• 3. Abunasser J, Metersky ML. A comparison of linezolid with glycopeptides in severe MRSA pneumonia. Expert Rev Anti Infect Ther. 2009 Oct;7(8):951-5.
• 4. Weigelt J, Itani K, Stevens D, Lau W, Dryden M, Knirsch C; Linezolid CSSTI Study Group. Linezolid versus vancomycin in treatment of complicated skin and soft tissue infections. Antimicrobial Agents and Chemotherapy. 2005 Jun;49(6):2260-6.
• 5. Wible K, Tregnaghi M, Bruss J, Fleishaker D, Naberhuis-Stehouwer S, Hilty M. Linezolid versus cefadroxil in the treatment of skin and skin structure infections in children. Pediatr Infect Dis J. 2003 Apr;22(4):315-23.
• 6. Lipsky BA, Itani K, Norden C; Linezolid Diabetic Foot Infections Study Group. Treating foot infections in diabetic patients: a randomized, multicenter, open-label trial of linezolid versus ampicillin-sulbactam/amoxicillin-clavulanate. Clin Infect Dis. 2004 Jan 1;38(1):17-24.
• 7. Weigelt J, Kaafarani HM, Itani KM, Swanson RN.Linezolid eradicates MRSA better than vancomycin from surgical-site infections. Am J Surg. 2004 Dec;188(6):760-6.

Published: November 16, 2009
Last updated: January 09, 2010