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Oxazolidinones

Oxazolidinones are modern group of antibacterial preparations. Currently only Linezolid is available in clinical practice. It is indicated for the treatment of infections caused by polyresistant gram-positive cocci.

Action mechanism
Oxazolidinones exert bacteriostatic action which is associated with inhibiting protein synthesis. Linezolid acts bactericidally against pneumococcus, B.fragilis and C.perfringens. Cross-resistance with other antibacterial preparations is not observed.

Spectrum of activity
Linezolid possesses antibacterial activity against the majority of aerobic and anaerobic gram-positive microorganisms including Staphylococcus spp. (MRSA and MRSE), Enterococcus spp. (including vancomycin resistant strains), S.pneumoniae, Streptococcus spp., Nocardia spp., Corynebacterium spp., L.monocytogenes, Clostridium spp., Peptostreptococcus spp.
Linezolid does not act on the majority of gram-negative microorganisms, however, exerts moderate activity against M.catarrhalis, H.influenzae, Legionella spp., N.gonorrhoeae, B.pertussis, F. meningosepticum, P.multocida as well as some gram-negative strains (Bacteroides spp., Prevotellaspp., F.nucleatum).

Indications
Oxazolidinones are used to treat:

  • Infections caused by multi-resistant gram-positive cocci (MRSA and MRSE; Enterococcus spp., including vancomycin resistant strains; S.pneumoniae, including PRA);
  • Complicated and uncomplicated infections of skin and soft tissues
  • Community-acquired and nosocomial pneumonia
  • Certain gram-negative infections in combination with other antibacterial preparations

Contraindications

  • Known reactions of hypersensitivity to Oxazolidones
  • Pregnancy
  • Breastfeeding

Side effects

  • The most common side effects associated with oxazolidinones applications include:
  • Digestive system: stomach pain, nausea, vomiting, diarrhea, taste changes
  • Hemopoietic system anemia, thrombocytopenia
  • Liver: increased activity of transaminases and alkaline phosphatase, increased level of bulirubin in the blood
  • CNS: headache

Cautions

  • Pregnancy. The safety of the medication has not been studied in pregnant women and therefore Linezolid and other oxazolidinones should not be used in this category of patients
  • Breastfeeding. There are no known if Linezolid pass through breast milk. Therefore the use of medication is not recommended
  • Blood. Linezolid may cause reversible anemia and/or thrombocytopenia (the risk if higher in prolonged therapy), so that patients with increased risk of bleeding, anemia and/or a history of thrombocytopenia, as well as in patients receiving anticoagulants or with linezolid therapy more than 2 weeks it is necessary to control platelet and hemoglobin levels

Drug interactions
Linezolid solution for infusion should not be mixed with ceftriaxone, amphoterecin B, diazepam, erythromycin, co-trimoxazole, phenytoin, pentamidine.
Linezolid is moderate MAO inhibitor, therefore it may enhance vasoconstrictive effects of dopamine, pseudoephedrine, phenyipropanolamine.

Information for patients
Linezolid tablets can be taken with or without food, before, during and after food intake. It is necessary to take the medication exactly as prescribed by your doctor. Consult your doctor if the symptoms of the disease does not improve within 7 days.