Linezolid (Zyvox) versus ...

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

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

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

Compared with other antibacterials, linezolid is associated with a high rate of 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 vs. Teicoplanin (Targocid)

Linezolid is superior to teicoplanin in the treatment of Gram-positive pneumonia, skin infections, and bacteremia (presence of bacteria in the bloodstream) 1, 9, 10.

The possible explanation of efficacy differences between teicoplanin and linezolid is superior skin and mucosal penetration of the latter 10.

Pneumonia

Linezolid provides better microbiological eradication in pneumonia caused by Methicillin-resistant Staphylococcus aureus (MRSA). However, the clinical efficacy and survival rates are similar to teicoplanin therapy9.

Results of comparison of teicoplanin and linezolid for MRSA pneumonia acquired from respiratory intensive care unit 9 Linezolid Teicoplanin
Bacteriological eradication rate
100%
72.7%
Mortality rate
42.1%
63.6%
mortality rate was lower in the linezolid group than the teicoplanin group, however this difference was not found statistically important

Gram-positive infections

Linezolid is clinically superior to teicoplanin in the treatment of Gram-positive infections 1, 10

Results of comparison of linezolid versus teicoplanin for Gram-positive infections in the critically ill 10 Linezolid Teicoplanin
Clinical success rate
71 patients of 100
(78.9%)
67 patients of 102
(72.8%)
Microbiological success rate
49 patients of 100
(70.0%)
45 patients of 102
(66.2%)
Adverse effects
similar
Intensive care unit mortality
similar
Success rates at short- and long-term follow-up
similar
Initial clearance of MRSA colonization (end of treatment)
51.1%
18.6%


Results study comparing linezolid with teicoplanin for suspected or proven Gram-positive infections 1 Linezolid Teicoplanin
Clinical cure rates at end of treatment in the intent-to-treat populations
95.5%
87.6%
Clinical cure rates by baseline diagnosis at end of treatment:
skin and soft tissue infection
96.6%
92.8%
pneumonia
96.2%
92.9%
bacteraemia
88.5%
56.7%
Bacterial eradication rate
81.9%
69.8%
Incidence of adverse events
30%
17%
Discontinuation rate due to drug related adverse events
4.7%
3.7%
The majority (9/13) of teicoplanin 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 failure.

Linezolid vs. Cefadroxil (Duricef)

Linezolid is as effective as cefadroxil in treating uncomplicated skin infections5.

In a randomized, blinded, multicenter trial comparing linezolid to cefadroxil for uncomplicated skin and soft tissue infections in children, clinical cure rates were similar (91% for linezolid and 90% for cefadroxil)5. Both treatments were well tolerated, with a comparable rate of serious side effects (0.8% for linezolid and 1.6% for cefadroxil).

Linezolid vs. Augmentin

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

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

Linezolid vs. Clarithromycin (Biaxin)

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

Linezolid vs. Daptomycin

Available limited data indicates that there is a trend toward increased survival with linezolid compared to daptomycin in the treatment of vancomycin-resistant enterococcal bloodstream infections15.

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Further reading

References
  • 1. Wilcox M, Nathwani D, Dryden M. Linezolid compared with teicoplanin for suspected or proven Gram-positive infections. J Antimicrob Chemother.. 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; Buenos Aires.
  • 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. Clin Infect Dis. 2004 Jan 1;38(1):17-24.
  • 8. Taşbakan MS, Korkmaz Ekren P, Pullukçu H, Başarık B, Susur A, Aydemir S, Başoğlu OK, Bacakoğlu F. Comparison of teicoplanin and linezolid therapies in patients with methicillin-resistant Staphylococcus aureus pneumonia acquired from respiratory intensive care unit. Mikrobiyol Bul. 2010 Jul;44(3):357-66. PubMed
  • 9. Cepeda JA, Whitehouse T, Cooper B, Hails J, Jones K, Kwaku F, Taylor L, Hayman S, Shaw S, Kibbler C, Shulman R, Singer M, Wilson AP. Linezolid versus teicoplanin in the treatment of Gram-positive infections in the critically ill: a randomized, double-blind, multicentre study. J Antimicrob Chemother. 2004 Feb;53(2):345-55. PubMed
  • 15. Whang DW, Miller LG, Partain NM, McKinnell JA. Systematic review and meta-analysis of linezolid and daptomycin for treatment of vancomycin-resistant enterococcal bloodstream infections. Antimicrob Agents Chemother. 2013 Oct;57(10):5013-8. PubMed

Published: November 16, 2009
Last updated: May 28, 2017

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