Linezolid and Tedizolid

ByBrian J. Werth, PharmD, University of Washington School of Pharmacy
Reviewed/Revised May 2024
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oxazolidinone antibiotics.

Linezolid

  • Streptococci

  • Enterococci, including vancomycin-resistant enterococci (VRE)

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

  • Mycobacteria, including Mycobacterium tuberculosis

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

Contraindications to Linezolid

Linezolid is contraindicated in patients who are taking monamine oxidase inhibitors (MAOIs).

Serotonin syndrome

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 medications with serotonergic activity

FAERS) suggests that linezolid is most likely to cause serotonin syndrome1). Subsequent data from cohort studies suggest that linezolid can likely safely be given to most patients taking antidepressants and opioids (2, 3). Thus, patients who are taking such medications and who urgently need linezolidcitalopram (or escitalopram) or methadone should be avoided when possible.

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

  • Those with uncontrolled hypertension

  • Those with thyrotoxicosis

  • Those with a pheochromocytoma

Contraindications references

  1. 1. Gatti M, Raschi E, De Ponti F. Serotonin syndrome by drug interactions with linezolid: clues from pharmacovigilance-pharmacokinetic/pharmacodynamic analysis. Eur J Clin Pharmacol. 2021;77(2):233-239. doi:10.1007/s00228-020-02990-1

  2. 2. Bai AD, McKenna S, Wise H, Loeb M, Gill SS. Association of Linezolid With Risk of Serotonin Syndrome in Patients Receiving Antidepressants. JAMA Netw Open. 2022;5(12):e2247426. Published 2022 Dec 1. doi:10.1001/jamanetworkopen.2022.47426

  3. 3. Mitwally H, Saad MO, Alkhiyami D, et al. Risk of serotonin syndrome in acutely ill patients receiving linezolid and opioids concomitantly: a retrospective cohort study. IJID Reg. 2022;5:137-140. Published 2022 Sep 24. doi:10.1016/j.ijregi.2022.09.008

Use of Linezolid During Pregnancy and Breastfeeding

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 of Linezolid

  • Reversible myelosuppression

  • Irreversible peripheral neuropathy

  • Reversible optic neuropathy

  • Serotonin syndrome

  • Reversible lactic acidosis

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

Tedizolid

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

Use of Tedizolid During Pregnancy and Breastfeeding

Tedizolid should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

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

More Information

The following English-language resource may be useful. Please note that THE MANUAL is not responsible for the content of this resource.

  1. FDA Adverse Events Reporting System (FAERS): A toll that allows users to query FAERS data

Drugs Mentioned In This Article

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