Linezolid (Zyvox) Antibiotic Side Effects, Dosage, and Mechanism of Action

  • Pharmacy Author:
    Omudhome Ogbru, PharmD

    Dr. Ogbru received his Doctorate in Pharmacy from the University of the Pacific School of Pharmacy in 1995. He completed a Pharmacy Practice Residency at the University of Arizona/University Medical Center in 1996. He was a Professor of Pharmacy Practice and a Regional Clerkship Coordinator for the University of the Pacific School of Pharmacy from 1996-99.

  • Medical Editor: Jay W. Marks, MD
    Jay W. Marks, MD

    Jay W. Marks, MD

    Jay W. Marks, MD, is a board-certified internist and gastroenterologist. He graduated from Yale University School of Medicine and trained in internal medicine and gastroenterology at UCLA/Cedars-Sinai Medical Center in Los Angeles.

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What is linezolid (Zyvox)? How does it work (mechanism of action)?

  • Linezolid (Zyvox) is a synthetic antibiotic that is effective against bacteria such as Enterococcus faecium, Staphylococcus aureus, Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, and others.
  • It is effective against Staphylococcus aureus isolates that are resistant to other antibiotics.
  • Linezolid prevents bacteria from growing by interfering with their ability to make proteins. Because proteins are made differently in people and bacteria, linezolid does not interfere with production of proteins in humans.
  • The FDA approved linezolid in April, 2000.

What are the uses for linezolid tablets?

Linezolid is used for treating these infections:

  • Nosocomial pneumonia caused by Staphylococcus aureus (methicillin-susceptible and -resistant isolates) or Streptococcus pneumoniae.
  • Community-acquired pneumonia caused by Streptococcus pneumoniae, or Staphylococcus aureus (methicillin-susceptible isolates only)
  • Complicated and uncomplicated skin and skin structure infections such as diabetic foot infections.
  • Vancomycin-resistant Enterococcus faecium infections.

What are the side effects of linezolid?

Common side effects of linezolid include:

Other possible side effects of linezolid include:

Possible serious side effects of linezolid include:

Cases of hypoglycemia have been reported during treatment with linezolid in patients with diabetes who are receiving insulin or oral hypoglycemic medications.

People who are taking drugs that may increase blood pressure should not receive linezolid or should be monitored closely for potential increases in blood pressure.

Linezolid should not be used for the treatment of catheter-related bloodstream infections or catheter-site infections since more people in the linezolid treated groups died in an investigational study of patients with these catheter-related bloodstream infections.

Like other antibiotics, linezolid may cause Clostridium difficile associated diarrhea or colitis.

Linezolid may suppress the bone marrow. Therefore, complete blood cell counts should be obtained weekly and discontinuation of treatment should be considered in patients who develop or have worsening bone marrow suppression.

Peripheral and optic neuropathy may occur, most often in patients treated for longer than 28 days. Patients who experience visual impairment should be evaluated immediately.

To reduce the risk of serotonin syndrome patients taking serotonergic antidepressants should only receive linezolid if other options are not available.

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What is the dosage for linezolid?

  • The recommended adult dose for treating pneumonia or complicated skin and skin structure infections is 600 mg orally or by intravenous infusion every 12 hours for 10 to 14 days.
  • Uncomplicated skin and skin structure infections are treated with 400 to 600 mg orally every 12 hours for 10 to 14 days.
  • The dose for vancomycin-resistant Enterococcus faecium infections is 600 mg orally or by intravenous infusion every 12 hours for 14 to 28 days.

Which drugs or supplements interact with linezolid?

  • Linezoild is a monoamine oxidase inhibitor (MAOI). This means that linezolid blocks the breakdown of compounds that are normally broken down my monoamine oxidase enzymes. This increases the levels of these compounds in the body and can increase the risk of side effects. Linezolid should not be used by patients taking monoamine oxidase inhibitors (MAOI) or within two weeks of taking an MAOI.
  • Linezolid should not be combined with antidepressants such as paroxetine (Paxil), fluoxetine (Prozac), amitriptyline, nortriptyline, bupropion (Wellbutrin, Zyban); pain medications like methadone, tramadol (Ultram), and meperidine (Demerol); dextromethorphan, St. John's Wort, cyclobenzaprine, and mirtazapine (Remeron). Such combinations lead to high serotonin levels, which may cause confusion, high blood pressure, tremor, hyperactivity, coma, and death.
  • Linezolid should not be combined with pseudoephedrine, phenylephrine, ephedrine, and phenylpropanolamine. The combination of linezolid and these drugs can cause an acute hypertensive episode.
  • Monoamine oxidase also breaks down tyramine, a chemical present in aged cheese, wines, and other aged foods. Since linezolid inhibits monoamine oxidase, it decreases the breakdown of tyramine from ingested food, thus increasing the level of tyramine in the body. Excessive tyramine can elevate blood pressure and cause a hypertensive crisis. Patients treated with MAOIs and lInezolid should adhere to recommended dietary modifications that reduce the intake of tyramine.

Is linezolid safe to take if I'm pregnant or breastfeeding?

Linezolid has not been adequately studied in pregnant women. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether linezolid is excreted in human milk.

What else should I know about linezolid?

What brand names are available for linezolid?

Zyvox is the brand name available for linezolid in the US.

Is linezolid available as a generic drug?

Linezolid is available in generic form.

Do I need a prescription for linezolid tablets?

Yes, you need a prescription from your doctor or pharmacist to obtain this drug.

  • Tablets: 600 mg;
  • Powder for Oral Suspension: 100 mg/5 ml;
  • Injection Solution: 200, 400, and 600 mg

How should I keep linezolid-oral tablets stored?

Linezolid should be stored at room temperature 25 C (77 F). Infusion bags should be kept in its overwrap and prevented from freezing.

REFERENCE: FDA Prescribing Information for linezolid.

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Reviewed on 8/29/2017
References
REFERENCE: FDA Prescribing Information for linezolid.

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