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Linezolid and Tedizolid

By Hans P. Schlecht, MD, MSc, Assistant Professor of Medicine, Department of Medicine, Division of Infectious Diseases & HIV Medicine, Drexel University College of Medicine
Christopher Bruno, MD, Assistant Professor of Medicine, Division of infectious Diseases & HIV Medicine, Drexel University College of Medicine

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Patient Education

Linezolid and tedizolid are oxazolidinone antibiotics (see Lincosamides, Oxazolidinones, and Streptogramins).


Linezolid is an oxazolidinone antibiotic that has activity against the following:

  • Streptococci

  • Enterococci (Enterococcus faecalis and E. faecium)

  • Staphylococci, including strains resistant to other classes of antibiotics

  • Mycobacteria

  • Anaerobes, such as Fusobacterium, Prevotella, Porphyromonas, and Bacteroides spp and peptostreptococci


Linezolid is contraindicated in patients with a prior allergic reaction to it.

Other contraindications include having risk factors for serotonin syndrome or hypertension.

Serotonin syndrome

Linezolid is a reversible, nonselective monamine oxidase inhibitor (MAOI); MAO inhibition causes levels of the neurotransmitter serotonin to increase. Thus, linezolid has the potential for causing serotonin syndrome (a hyperserotonergic state characterized by mental status changes, neurologic abnormalities, and autonomic instability—see also Serotonin Syndrome) when it is used in patients with either of the following: .

Such drugs include SSRIs, MAOIs (eg, phenelzine, isocarboxazid), tricyclic antidepressants, serotonin 1B,1D receptor agonists (triptans), meperidine, bupropion, and buspirone. Patients who are taking such drugs and urgently need linezolid may be treated if the benefit is thought to outweigh the risk and if they

  • Promptly stop the proserotonergic drug

  • Are carefully monitored for manifestations of serotonin syndrome for 2 wk after stopping the drug (for fluoxetine, 5 wk) or for 24 h after the last linezolid dose

Linezolid is not been studied in patients with carcinoid syndrome; it should be used only if patients are closely monitored for symptoms and signs of serotonin syndrome.


Linezolid should not be given to the following patients unless they are monitored for potential increases in BP:

  • Those taking any of the following: sympathomimetic drugs (eg, pseudoephedrine), vasopressors (eg, epinephrine, norepinephrine), or dopaminergic drugs (eg, dopamine, dobutamine)

  • Those with uncontrolled hypertension

  • Those with thyrotoxicosis

  • Those with a pheochromocytoma

Use During Pregnancy and Breastfeeding

Linezolid is in pregnancy category C (animal studies show some risk, evidence in human studies is inadequate, but clinical benefit sometimes exceeds risk).

Whether linezolid is excreted in breast milk or is safe to use during breastfeeding is unknown.

Adverse Effects

Adverse effects include

  • Reversible myelosuppression

  • Irreversible peripheral neuropathy

  • Reversible optic neuropathy

  • Serotonin syndrome

Reversible myelosuppression, including thrombocytopenia, leukopenia, and anemia, occurs in about 3% of patients, usually when therapy is used > 2 wk. Consequently, CBC is monitored weekly, especially when therapy lasts > 2 wk.

Peripheral and optic neuropathy may occur with prolonged use, and patients taking long-term linezolid therapy should be closely monitored for these disorders.


Tedizolid is an oxazolidinone antibiotic with a spectrum of activity similar to that of linezolid, although it may have activity against some linezolid-resistant gram-positive cocci.

In clinical trials, risk of serotonin syndrome and thrombocytopenia was lower with tedizolid than with linezolid. Tedizolid can cause significant neutropenia and its use is not recommended in patients with neutrophil counts of < 1000 cell/mm3.

Drugs Mentioned In This Article

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