Oxazolidinones are a unique class of synthetic antibiotics that have a low potential for development of antibacterial resistance. They are widely used in the USA, Australia and the European countries.
Antibiotics of this group provide predominantly bacteriostatic effect. Their action is different from the mechanism of action of other antimicrobial drugs.
Oxazolidinones work by inhibiting protein synthesis in the bacterial cell ribosomes. Due to this mechanism of action, the risk of developing cross-resistance is reduced.
Today, the oxazolidinones group includes two drugs:
is the first representative of oxazolidinones. This drug was approved by the FDA for the treatment of infections caused by multi-resistant flora, in particular methicillin-resistant Staphylococcus aureus (MRSA).
Linezolid is also used to treat infections caused by vancomycin-resistant enterococci (VRE).
is the second drug of the oxazolidinones group. It was approved by the FDA about 10 years after Linezolid approval. This drug has improved microbiological properties and in certain cases may have an activity against some linezolid-resistant gram-positive cocci.
The spectrum of antimicrobial activity of oxazolidinones includes the following aerobic and facultative gram-positive bacteria:
- S. lugdunensis
- E. faecalis
Oxazolidinones are not used to treat infectious diseases caused by gram-negative bacteria. Herewith, it was found that Linezolid has activity against such gram-negative bacterium as Pasteurella multocida causing soft tissue infection in humans.
It has been clinically proven that oxazolidinones have effective bacteriostatic and significant post-antibiotic effects against the sensitive microflora.
Moreover, antimicrobial drugs of this group have low toxicity and favorable safety profile that makes it possible to use them in patients with hepatic and renal insufficiency of varying severity.
Linezolid is recommended for the treatment of bacterial infections of various localization in adults and pediatric patients, including newborns. Tedizolid is used only in patients aged 18 years and older.
Indications for the use of antimicrobial agents are:
- Community- and hospital-acquired pneumonia;
- Vancomycin-resistant Enterococcus faecium infections, including cases with concurrent bacteremia (UTI, endocarditis);
- Uncomplicated and complicated skin and skin structure infections (diabetic foot, pasteurellosis, necrotizing fasciitis, and phlegmon).
- Acute bacterial skin and skin structure infections caused by Gram-positive microorganisms (cellulitis, erysipelas, wound infection, and skin abscesses).
Dosage forms of Oxazolidinones very well penetrate into the skin, soft tissues, heart, intestines, urine and kidneys. An antimicrobial drug of this group is well penetrated in the synovial fluid, bladder, bile and bones.
Tedizolid is one of the most effective antibacterial drugs for the treatment of acute infections of the skin and soft tissues, including those that are caused by resistance to other antibiotics.
To date, Linezolid is the only antibiotic that can be prescribed orally for the treatment of infections caused by multi-resistant strains of Staphylococcus aureus and enterococci.
In a number of cases, Linezolid is an effective alternative to Vancomycin antibiotic. The antimicrobial drug has a favorable safety profile and it is well tolerated by patients of all age groups.