Linezolid is a synthetic antibiotic, the first of the oxazolidinone class, used for the treatment of infections caused by multi-resistant bacteria. The drug works by inhibiting the initiation of bacterial protein synthesis.
- Skin and soft tissue infections
- Treat tuberculosis.
- febrile neutropenia
- Infections of the central nervous system
600 mg IV or orally every 12 hours for 14 to 28 days
It has in vitro activity against aerobic Gram positive bacteria, certain Gram negative bacteria and anaerobic microorganisms. It selectively inhibits bacterial protein synthesis through binding to sites on the bacterial ribosome and prevents the formation of a functional 70S-initiation complex. which is an essential component of the bacterial translation process. The results of time-kill studies have shown linezolid to be bacteriostatic.
Linezolid is rapidly and extensively absorbed after oral dosing. Maximum plasma concentrations are reached approximately 1 to 2 hours after dosing, and the absolute bioavailability is approximately 100%.
40 to 50 L [healthy adult volunteers] ,protein binding 31%
Linezolid is primarily metabolized by oxidation of the morpholine ring, which results in two inactive ring-opened carboxylic acid metabolites: the aminoethoxyacetic acid metabolite (A), and the hydroxyethyl glycine metabolite
80% of the administered dose is excreted through urine. About 30% of the drug is excreted in unchanged form and 50% of the drug is excreted in the form of metabolites. 9% of the drug is excreted in feces. In accordance with total clearance 50% of the drug excreted is nonrenal
- Hypersensitive patients
- Concomitant use of linezolid with MAO inhibitors
- Long use of drug causes myelosuppression
- In treatment with linezolid peripheral and optic neuropathies occurs
- Visual defects also occurs
- Serotonin Syndrome
- Clostridium difficile associated diarrhea