Everything about Linezolid totally explained
Linezolid (
INN) is a synthetic
antibiotic, the first of the
oxazolidinone class, used for the treatment of infections caused by multi-resistant
bacteria including
streptococcus and
methicillin-resistant Staphylococcus aureus (MRSA). It is marketed under the trade name
Zyvox (or
Zyvoxid in
Europe) (
Pfizer).
Linezolid was the first commercially available
oxazolidinone antibiotic. Therapy using linezolid can be quite expensive, with prices for a course of treatment ranging up to several thousands of dollars.
Usage
It is usually reserved for the treatment of serious
bacterial infections where older antibiotics have failed due to
antibiotic resistance. Conditions such as skin infections or nosocomial
pneumonia where
methicillin or
penicillin resistance is found are indicators for linezolid use.
Linezolid is effective against
gram-positive pathogens, notably
Enterococcus faecium,
Staphylococcus aureus,
Streptococcus agalactiae,
Streptococcus pneumoniae, and
Streptococcus pyogenes. It has almost no effect on gram-negative bacteria and is only
bacteriostatic against most
Enterococcus species. Linezolid also provides some anaerobic coverage.
Linezolid has been used to treat
tuberculosis.
History
The oxazolidinone class was discovered by researchers at E.I. duPont de Nemours and reported in
1987.
Upjohn developed linezolid (Upjohn is now part of
Pfizer) and
Food and Drug Administration (FDA) approval was granted in
April of
2000. It is sold in the U.S. under the tradename
Zyvox in either tablet form, oral suspension powder, or in an inactive medium for intravenous injection.
Initially there was hope that bacteria would be unable to develop resistance to it. However, in 2001
Staphylococcus aureus was first identified as being resistant to linezolid.
Mechanism of Action
Linezolid works on the initiation of protein synthesis. It does this by stopping the
30S and
50S subunits of the ribosome from binding together. Linezolid binds on the 23S portion of the 50S subunit close to the peptidyl transferase and
chloramphenicol binding sites. This then stops the interaction with the 30S subunit.
Dosing
The adult dose of linezolid is 600mg twice daily orally or intravenously for a maximum of 14 days. The dose in children is 10mg/kg orally or intravenously three times a day for a maximum of 14 days.
Linezolid has been used in the treatment of
tuberculosis (in combination with other drugs). or 600mg twice daily have both been used to good effect. The treatment often needs to be continued for many months and the rate of adverse effects is high. The anemia and thrombocytopenia caused by linezolid are not prevented by concurrent administration of
pyridoxine 125mg daily.
Linezolid is a weak
monoamine oxidase inhibitor (MAOI) and can't be used with
tyramine containing foods or
pseudoephedrine.
Linezolid is toxic to
mitochondria (probably because of the similarity between mitochondrial and bacterial
ribosomes). Signs of mitochondrial toxicity include
lactic acidosis and
peripheral neuropathy. Painful sensory neuropathy.
Further Information
Get more info on 'Linezolid'.
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