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Linezolid
U.S. Brand Names
Pharmacological Index
Use
Pregnancy Risk Factor
Pregnancy/Breast-Feeding Implications
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Administration
Monitoring Parameters
Patient Information
Nursing Implications
Dosage Forms

U.S. Brand Names
Zyvox™

Pharmacological Index

Antibiotic, Oxazolidinone


Use

Treatment of vancomycin-resistant Enterococcus faecium (VRE) infections, nosocomial pneumonia caused by Staphylococcus aureus including MRSA or Streptococcus pneumoniae (penicillin-susceptible strains only), complicated and uncomplicated skin and skin structure infections, and community-acquired pneumonia caused by susceptible gram-positive organisms.


Pregnancy Risk Factor

C


Pregnancy/Breast-Feeding Implications

Should be used in pregnancy only if the potential benefit justifies the risk to the fetus. It is unknown if excreted in human milk. Use cautiously if administered to a breast-feeding woman.


Contraindications

Allergy to linezolid or any other component


Warnings/Precautions

Linezolid has mild monoamine oxidase inhibitor properties and has the potential to have the same interactions as other MAOIs; use with caution in uncontrolled hypertension, pheochromocytoma, carcinoid syndrome, or untreated hyperthyroidism; thrombocytopenia has been reported and may be dependent on duration of therapy (generally >2 weeks of treatment); avoid use with serotonergic agents such as TCAs, venlafaxine, trazodone, sibutramine, meperidine, dextromethorphan, and SSRIs; consider alternatives before initiating outpatient treatment (unnecessary use may lead the development of resistance to linezolid)


Adverse Reactions

1% to 10%:

Cardiovascular: Hypertension (1% to 3%)

Central nervous system: Headache (0.5% to 11%), insomnia (3%), dizziness (0.4% to 2%), fever (2%)

Dermatologic: Rash (2%)

Gastrointestinal: Nausea (3% to 10%), diarrhea (3% to 11%), vomiting (1% to 4%), constipation (2%), taste alteration (1% to 2%), tongue discoloration (0.2% to 1%), oral moniliasis (0.4% to 1%), pancreatitis

Genitourinary: Vaginal moniliasis (1% to 2%)

Hematologic: Thrombocytopenia (0.3% to 10%), anemia, leukopenia, neutropenia

Hepatic: Abnormal LFTs (0.4% to 1%)

Miscellaneous: Fungal infections (0.1% to 2%)

<1%: C.difficile-related complications, increase in creatinine, dyspepsia, localized abdominal pain, pruritus


Overdosage/Toxicology

Treatment includes supportive care; hemodialysis may improve elimination (30% of a dose is removed during a 3-hour hemodialysis session)


Drug Interactions

Linezolid is a reversible, nonselective inhibitor of MAO. Serotonergic agents (eg, TCAs, venlafaxine, trazodone, sibutramine, meperidine, dextromethorphan, and SSRIs) may cause a serotonin syndrome (eg, hyperpyrexia, cognitive dysfunction) when used concomitantly. Adrenergic agents (eg, phenylpropanolamine, pseudoephedrine, sympathomimetic agents, vasopressor or dopaminergic agents) may cause hypertension.


Stability

Store at 25°C (77°F). Protect from light. Keep infusion bags in overwrap until ready for use. Protect infusion bags from freezing. Use reconstituted suspension within 21 days.


Mechanism of Action

Inhibits bacterial protein synthesis by binding to bacterial 23S ribosomal RNA of the 50S subunit. This prevents the formation of a functional 70S initiation complex that is essential for the bacterial translation process. Linezolid is bacteriostatic against enterococci and staphylococci and bactericidal against most strains of streptococci.


Pharmacodynamics/Kinetics

Absorption: Rapid and extensive

Distribution: Steady state Vd 40-50 L

Protein binding: 31%

Metabolism: Hepatic by oxidation of the morpholine ring which results in 2 inactive metabolites (aminoethoxyacetic acid, hydroxyethyl glycine). Does not involve cytochrome P450 isoenzymes.

Bioavailability: 100%

Half-life: 4-5 hours

Time to peak: 1-2 hours

Elimination: 65% nonrenal for linezolid; 30% renally as linezolid


Usual Dosage

Adult:

VRE infections: 600 mg every 12 hours for 14-28 days

Nosocomial pneumonia, complicated skin and skin structure infections, community-acquired pneumonia including concurrent bacteremia: 600 mg every 12 hours for 10-14 days

Oral: Uncomplicated skin and skin structure infections: 400 mg every 12 hours for 10-14 days

Dosage adjustment in renal impairment: No specific adjustment recommended. The two primary metabolites may accumulate in patients with renal impairment but the clinical significance is unknown. Weigh the risk of accumulation of metabolites versus the benefit of therapy. Both linezolid and the two metabolites are eliminated by dialysis. Linezolid should be given after hemodialysis.

Dosage adjustment in hepatic impairment: No dosage adjustment required for mild to moderate hepatic insufficiency (Child-Pugh class A or B). Use in severe hepatic insufficiency has not been adequately evaluated.

Elderly: No dosage adjustment required


Dietary Considerations

Take with or without food. Suspension contains 20 mg phenylalanine per teaspoonful.


Administration

Administer intravenous infusion over 30-120 minutes. Do not mix or infuse with other medications. The yellow color of the injection may intensify over time without affecting potency.


Monitoring Parameters

Platelet counts in patients at increased risk of bleeding, with pre-existing thrombocytopenia, on concomitant medications that decrease platelet count or function, or in those who require >2 weeks of therapy.


Patient Information

Take with or without food. Take with food if medicine causes stomach upset. Tell your healthcare provider if you have hypertension or are taking any cold remedy or decongestant. Limit quantities of tyramine-containing foods. Gently mix suspension. Store at room temperature.


Nursing Implications

Administer intravenous infusion over 30-120 minutes. Do not mix or infuse with other medications. The yellow color of the injection may intensify over time without affecting potency.


Dosage Forms

Infusion: 200 mg (100 mL); 400 mg (200 mL); 600 mg (300 mL)

Suspension, oral (orange-flavored): 20 mg/mL (150 mL)

Tablet: 400 mg, 600 mg


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