Linezolid (brand name, Zyvox) is an antibiotic used to treat methicillin-resistant Staphylococcus aureus (MRSA) infections in people with cystic fibrosis (CF). The number of MRSA infections, which are highly resistant, is increasing in people with this disease, and is associated with delayed recovery from exacerbations and accelerated decline of lung function in children with CF.1
History of linezolid
Linezolid was the first in a new class of synthetic antibiotics known as oxazolidinones. Oxazolidinones were discovered in the late 1970s, and of immediate interest because they showed activity against methicillin-resistant organisms. But their development soon stopped because of findings of liver toxicity, and it was only 1990s that these class of antibiotics was re-investigated. Linezolid was discovered in 1996.
Oxazolidinones are the only new class of antibiotics introduced into clinical practice since the mid-1970s.2
How linezolid works
Linezolid has a unique structure and mechanism of action that targets bacterial protein production (or synthesis) in its earliest stages — that of initial bacterial protein synthesis. Bacteria can’t multiply if proteins are not produced, and ultimately they die.
In gram-positive bacteria, which includes Staphylococcus aureus, Linezolid is also thought to inhibit the expression of virulence factors and decrease toxin production. It stops the growth of enterococci and staphylococci, and kills most streptococci.2 (Linezolid is not active against gram-negative pathogens.)
Other details about linezolid
Linezolid may be taken by mouth (tablet or liquid) or be given by intravenous injection, and its oral form is usually taken with food twice-daily for 10 to 28 days. The length of the treatment depends on the type of infection.
Side effects of linezolid can include diarrhea, headache, nausea, vomiting and stomach pain, vaginal itching or discharge, sleeping problems, dizziness, white patches in the mouth, and change in the color of the tongue.3,4
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