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Linezolid and Tedizolid

By

Brian J. Werth

, PharmD, University of Washington School of Pharmacy

Last full review/revision May 2020| Content last modified May 2020
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NOTE: This is the Professional Version. CONSUMERS: Click here for the Consumer Version

Linezolid and tedizolid are oxazolidinone antibiotics.

Linezolid

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

  • Enterococci, including vancomycin-resistant enterococci (VRE)

  • Staphylococci, including methicillin-resistant S. aureus (MRSA) and other strains resistant to other classes of antibiotics

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

Contraindications

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) when it is used in patients with either of the following:

  • Endocrinologically active carcinoid tumors

  • Use of drugs with serotonergic activity

Such drugs include selective serotonin reuptake inhibitors, 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 weeks after stopping the drug (for fluoxetine, 5 weeks) or for 24 hours after the last linezolid dose

Linezolid has 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.

Hypertension

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

  • 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

Animal reproduction studies with linezolid show some risk, and no adequate, well-controlled studies have been done in pregnant women. Linezolid should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

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

Adverse Effects

Adverse effects of linezolid include

  • Reversible myelosuppression

  • Irreversible peripheral neuropathy

  • Reversible optic neuropathy

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

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

Tedizolid

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, like linezolid, can cause significant neutropenia, and the use of these oxazolidinone antibiotics is not recommended in patients with neutrophil counts of < 1000 cell/mcL (< 1 × 109/L) when acceptable alternatives exist.

Use During Pregnancy and Breastfeeding

Animal reproduction studies with tedizolid show some risk, and no adequate and well-controlled studies have been done in pregnant women. Tedizolid should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

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

Click here for Patient Education
NOTE: This is the Professional Version. CONSUMERS: Click here for the Consumer Version
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