|
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 |
|
Copyright © 1978-2000 Lexi-Comp Inc. All Rights Reserved
|