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Linezolid and Tedizolid

By

Brian J. Werth

, PharmD, University of Washington School of Pharmacy

Last full review/revision May 2020
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Linezolid

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

Contraindications to Linezolid

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

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 Serotonin Syndrome Serotonin syndrome is a potentially life-threatening condition resulting from increased central nervous system serotonergic activity that is usually drug related. Symptoms may include mental... read more (a hyperserotonergic state characterized by mental status changes, neurologic abnormalities, and autonomic instability) when it is used in patients with either of the following:

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 of Linezolid

Adverse effects of linezolid include

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.

Drugs Mentioned In This Article

Drug Name Select Trade
No US brand name
CLEOCIN
CUBICIN
FLAGYL
MONUROL
ZYVOX
VIBATIV
DALVANCE
SIVEXTRO
ORBACTIV
BACTROBAN
AZACTAM
VANCOCIN
TINDAMAX
FORTAZ, TAZICEF
ZITHROMAX
BIAXIN
ERY-TAB, ERYTHROCIN
DIFICID
No US brand name
No US brand name
GENOPTIC
ANCEF, KEFZOL
FURADANTIN, MACROBID, MACRODANTIN
KEFLEX
THAM
No US brand name
CEFOTAN
MEFOXIN
No US brand name
CEFTIN, ZINACEF
No US brand name
No US brand name
SUPRAX
CLAFORAN
No US brand name
No US brand name
No US brand name
MAXIPIME
No US brand name
BACIIM
TYGACIL
ACHROMYCIN V
MINOCIN
BICILLIN L-A
No US brand name
PRIMSOL
MYCOBUTIN
VIBRAMYCIN
XERAVA
RIFADIN, RIMACTANE
No US brand name
PRIFTIN
XIFAXAN
DORIBAX
INVANZ
MERREM
AMOXIL
SULFAMYLON
No US brand name
BLEPH-10
No US brand name
NALLPEN IN PLASTIC CONTAINER
BACTOCILL IN PLASTIC CONTAINER
AZULFIDINE
BACTRIM, SEPTRA
DARAPRIM
SILVADENE
QUALAQUIN
CILOXAN, CIPRO
No US brand name
ZEMDRI
No US brand name
TOBI, TOBREX
No US brand name
NUZYRA
No US brand name
COLY-MYCIN M
ARALEN
PROGRAF
TIKOSYN
SEROQUEL
LANOXIN
OZURDEX
DILANTIN
LANIAZID
No US brand name
NARDIL
MARPLAN
DEMEROL
WELLBUTRIN, ZYBAN
No US brand name
SYNERCID
PROZAC, SARAFEM
ELIXOPHYLLIN
ANTABUSE
COUMADIN
ACZONE
No US brand name
No US brand name
OCUFLOX
AFRINOL, SUDAFED
ADRENALIN
LEVOPHED
BAXDELA
FACTIVE
LEVAQUIN
AVELOX
No US brand name
No US brand name
ZYMAR
No US brand name
ORAP
ZOSYN
CORTEF, SOLU-CORTEF
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