Linezolid

Mode of Action:

Linezolid binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex, which is essential for bacterial reproduction.

Drug Label Information | Brands:

Brands Linezolid in Kenya:

Arlin®, Beximco Pharmaceuticals Ltd
Bactolid®, Hetero Labs Ltd
Linospa®, Cipla
Linzo® , Medisel Kenya Limited.
Lizolid®, Glenmark Pharmaceuticals Limited
Lizomac®, Macleods Pharmaceuticals Limited
Lizomed®, Aglowmed Limited
Zyvox®, Pfizer

INDICATIONS:

Linezolid is indicated for the treatment of infections caused by susceptible strains of the designated microorganisms in the specific conditions listed below. Linezolid is not indicated for the treatment of Gram-negative infections. It is critical that specific Gram-negative therapy be initiated immediately if a concomitant Gram-negative pathogen is documented or suspected

Pneumonia

Nosocomial pneumonia caused by Staphylococcus aureus (methicillin-susceptible and -resistant isolates) or Streptococcus pneumoniae

Community-acquired pneumonia caused by Streptococcus pneumoniae, including cases with concurrent bacteremia, or Staphylococcus aureus (methicillin-susceptible isolates only)

Skin and Skin Structure Infections

Complicated skin and skin structure infections, including diabetic foot infections, without concomitant osteomyelitis, caused by Staphylococcus aureus (methicillin-susceptible and -resistant isolates), Streptococcus pyogenes, or Streptococcus agalactiae. Linezolid  has not been studied in the treatment of decubitus ulcers

Uncomplicated skin and skin structure infections caused by Staphylococcus aureus (methicillin-susceptible isolates only) or Streptococcus pyogenes.

Vancomycin-resistant Enterococcus faecium Infections

Vancomycin-resistant Enterococcus faecium infections, including cases with concurrent bacteremia

CONTRAINDICATIONS:

Known hypersensitivity to linezolid or any of the other product components.

Patients taking any monoamine oxidase inhibitors (MAOI) or within two weeks of taking an MAOI.

ADVERSE DRUG REACTIONS:

Most common adverse reactions (>5% of adult and/or pediatric patients treated with linezolid) include: diarrhea, vomiting, headache, nausea, and anemia

DRUG INTERACTIONS:

Monoamine Oxidase Inhibitors

Linezolid is a reversible, nonselective inhibitor of monoamine oxidase.

Adrenergic and Serotonergic Agents

Linezolid has the potential for interaction with adrenergic and serotonergic agents.

WARNINGS AND PRECAUTIONS

  • Myelosuppression: Monitor complete blood counts weekly. Consider discontinuation in patients who develop or have worsening myelosuppression.
  • Peripheral and optic neuropathy: Reported primarily in patients treated for longer than 28 days. If patients experience symptoms of visual impairment, prompt ophthalmic evaluation is recommended.
  • Serotonin syndrome: Patients taking serotonergic antidepressants should receive linezolid only if no other therapies are available. Discontinue serotonergic antidepressants and monitor patients for signs and symptoms of both serotonin syndrome and antidepressant discontinuation.
  • A mortality imbalance was seen in an investigational study in linezolid-treated patients with catheter-related bloodstream infections.
  • Clostridium difficile associated diarrhea: Evaluate if diarrhea occurs.
  • Potential interactions producing elevation of blood pressure: monitor blood pressure.
  • Hypoglycemia: Postmarketing cases of symptomatic hypoglycemia have been reported in patients with diabetes mellitus receiving insulin or oral hypoglycemic agents.