Linezolid: Indications, Dosage, Mechanism of Action and Side Effects

Indications

Linezolid a synthetic oxazolidinone antimicrobial drug belongs to the class of antibiotics. It is used primarily for infections caused by gram-positive bacteria or gram-positive bacteria that are resistant to other antibiotics. Linezolid is approved by the FDA for the treatment of:

(1) skin and soft tissue infections (SSTI)

(2) Bacterial pneumonia

(3) Vancomycin-resistant enterococci (VRE) infections

Off-label treatments for other diseases include:

(4) Anthrax

(5) Brain infections (brain abscesses, meningitis, subdural fluid and ventriculitis)

(6) Bone or/and joint infections (osteomyelitis, infectious arthritis, orthopaedic device-related infections)

(7) Septicaemia

(8) Other infections (febrile neutropenia)

Dosage

Linezolid is available in 600 mg tablets, 100 mg/5 mL oral suspension, and 2 mg/mL injection.

Administration: IV infusion for 30-120 min; avoid mixing with other meds. Flush IV line before and after. Color change in injection is normal and does not affect efficacy.

Adult Dosage:

Bacterial pneumonia: 600 mg IV/oral q12h for 10-14 days.

Community-Acquired Pneumonia with Bacteremia: Same as nosocomial.

Complicated Skin Infections (cSSTIs): 600 mg IV/oral q12h for 10-14 days.

Uncomplicated Skin Infections: 400 mg oral q12h for 10-14 days.

VRE Infections: 600 mg IV/oral q12h for 14-28 days.

Mechanism of Actiond

Linezolid exerts its antimicrobial effect by inhibiting bacterial protein synthesis. linezolid attaches to a site on the 50S subunit of bacterial 23S ribosomal RNA and prevents the formation of a functional 70S initiation complex, which interferes with the process of protein translation and thus inhibits protein synthesis. It also prevents the expression of virulence components, thereby reducing the production of toxins by Gram-positive pathogens.

Side Effects

Common side effects of Linezolid include dizziness, headache, nausea, vomiting, diarrhoea, rash, discolouration of the tongue, changes in vision, and seizures. Biochemical markers may also show a decrease in platelets, haemoglobin, white blood cell count, elevated pancreatic enzymes, and elevated liver function test results. Severe cases may result in abnormal bleeding or bruising, severe diarrhoea, lactic acidosis, hypertension and neuropathy. Severe allergic reactions are rare. Contact your doctor if any of these serious adverse reactions occur.

References:

[1] SEYED MOHAMMAD REZA HASHEMIAN  Mojdeh G  Tayebeh Farhadi. Linezolid: a review of its properties, function, and use in critical care.[J]. Drug Design, Development and Therapy, 2018: 1759-1767. DOI:10.2147/DDDT.S164515.

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