Products
Linezolid is commercially available as an infusion solution, in the form of film-coated tablets, and as granules for preparation of a suspension (Zyvoxid, generics). It has been approved in many countries since 2001.
Structure and properties
Linezolid (C16H20FN3O4, Mr = 337.3 g/mol) was the first agent developed from the oxazolidinone group. It is structurally closely related to rivaroxaban (Xarelto).
Effects
Linezolid (ATC J01XX08) has antibacterial properties against aerobic Gram-positive bacteria, some Gram-negative and anaerobic microorganisms. The effects are based on inhibition of protein synthesis by binding to bacterial ribosomes. Unlike other antibiotics, it is effective at the beginning of translation and inhibits the formation of the initiation complex. The half-life is approximately 5 to 7 hours.
Indications
For the treatment of selected bacterial infectious diseases, particularly nosocomial pneumonias and complicated skin and soft tissue infections (including those with , , , , ).
Dosage
According to the SmPC. Peroral dosage forms are taken twice daily, independent of meals.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Linezolid is a weak, reversible, and nonselective MAO inhibitor, and corresponding drug-drug interactions are possible. In contrast, it does not interact with CYP450 isoenzymes.
Adverse effects
The most common possible adverse effects include digestive disturbances such as diarrhea, nausea, vomiting, cramps, and flatulence; hyperglycemia; headache; taste changes (metallic taste); and fungal infections. Rarely, lactacidosis and serotonin syndrome may occur.
