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Linezolid

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Abstract

  • ▴ Linezolid is an oxazolidinone antibacterial agent that acts by inhibiting the initiation of bacterial protein synthesis. Cross-resistance between linezolid and other inhibitors of protein synthesis has not been demonstrated.

  • ▴ Linezolid has a wide spectrum of activity against Gram-positive organisms including methicillin-resistant staphylococci, penicillin-resistant pneumococci and vancomycin-resistant Enterococcus faecalis and E. faecium. Anerobes such as Clostridium spp., Peptostreptococcus spp. and Prevotella spp. are also susceptible to linezolid.

  • ▴ Linezolid is bacteriostatic against most susceptible organisms but displays bactericidal activity against some strains of pneumococci, Bacteroides fragilis and C. perfringens.

  • ▴ In clinical trials involving hospitalised patients with skin/soft tissue infections (predominantly S. aureus), intravenous/oral linezolid (up to 1250mg mg/day) produced clinical success in >83% of individuals. In patients with community-acquired pneumonia, success rates were >94%.

  • ▴ Preliminary clinical data also indicate that twice daily intravenous/oral linezolid 600mg is as effective as intravenous vancomycin 1g in the treatment of patients with hospital-acquired pneumonia and in those with infections caused by methicillin-resistant staphylococci. Moreover, linezolid 600mg twice daily produced >85% clinical/microbiological cure in vancomycin-resistant enterococcal infections.

  • ▴ Linezolid is generally well tolerated and gastrointestinal disturbances are the most commonly occurring adverse events. No clinical evidence of adverse reactions as a result of monoamine oxidase inhibition has been reported.

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Notes

  1. Both low and high dosage regimens were switched from three times daily to twice daily, maintaining the same total daily dosage, after interim pharmacokinetic data became available.

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  1. Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, Auckland, 10, New Zealand

    Delyth Clemett & Anthony Markham

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  2. Anthony Markham
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Clemett, D., Markham, A. Linezolid. Drugs 59, 815–827 (2000). https://doi.org/10.2165/00003495-200059040-00007

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