Linezolid and tedizolid are oxazolidinone antibiotics Lincosamides, Oxazolidinones, and Streptogramins Lincosamides ( clindamycin), oxazolidinones ( linezolid, tedizolid), and streptogramins ( dalfopristin [streptogramin A] and quinupristin [streptogramin B]) are structurally different but are... read more 
.
Linezolid
Linezolid is an oxazolidinone antibiotic that has activity against the following:
Staphylococci Staphylococcal Infections Staphylococci are gram-positive aerobic organisms. Staphylococcus aureus is the most pathogenic; it typically causes skin infections and sometimes pneumonia, endocarditis, and osteomyelitis... read more
, including methicillin-resistant S. aureus (MRSA) and other strains resistant to other classes of antibioticsAnaerobes Overview of Anaerobic Bacteria Bacteria can be classified by their need and tolerance for oxygen: Facultative: Grow aerobically or anaerobically in the presence or absence of oxygen Microaerophilic: Require a low oxygen concentration... read more , such as Fusobacterium, Prevotella, Porphyromonas, and Bacteroides species and peptostreptococci
Contraindications to Linezolid
Linezolid is contraindicated in patients with a prior allergic reaction to it.
Linezolid is contraindicated in patients who are taking monamine oxidase inhibitors (MAOIs).
Serotonin syndrome
Linezolid is a reversible, nonselective 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:
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 of Linezolid
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 cells/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 |
|---|---|
linezolid |
Zyvox, Zyvox Powder, Zyvox Solution |
tedizolid |
SIVEXTRO |
vancomycin |
FIRVANQ, Vancocin, Vancocin Powder, VANCOSOL |
phenelzine |
Nardil |
isocarboxazid |
Marplan |
meperidine |
Demerol, Meperitab |
bupropion |
Aplenzin, Budeprion SR , Budeprion XL , Buproban, Forfivo XL, Wellbutrin, Wellbutrin SR, Wellbutrin XL, Zyban |
buspirone |
BuSpar, Buspar Dividose |
fluoxetine |
Prozac, Prozac Weekly, Sarafem, Selfemra |
pseudoephedrine |
Contac Cold 12 Hour, Dimetapp Decongestant, Drixoral, ElixSure Cold, ElixSure Congestion, Entex, Genaphed , KidKare , Myfedrine, NASAL Decongestant, Nasofed, Nexafed, PediaCare Infants' Decongestant, Pseudo-Time, Silfedrine, Sudafed, Sudafed 12 Hour, Sudafed 24 Hour, Sudafed Children's Nasal Decongestant, Sudafed Congestion, Sudafed Sinus Congestion, Sudogest, Sudogest 12 Hour, Sudogest Children's , Tylenol Children's Simply Stuffy, Zephrex-D |
epinephrine |
Adrenaclick, Adrenalin, Auvi-Q, Epifrin, EpiPen, Epipen Jr , Primatene Mist, SYMJEPI, Twinject |
norepinephrine |
Levophed |
dopamine |
Intropin |
dobutamine |
Dobutrex |
