THE MERCK MANUAL MEDICAL LIBRARY: The Merck Manual of Diagnosis and Therapy
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Linezolid Drug Information Provided by Lexi-Comp

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This information has been developed and provided by an independent third-party source. Merck & Co., Inc. does not endorse and is not responsible for the accuracy of the content, or for practices or standards of non-Merck sources.

Medication Safety Issues

Sound-alike/look-alike issues:

Zyvox® may be confused with Ziox™, Zosyn®, Zovirax®

Pronunciation

(li NE zoh lid)

U.S. Brand Names

  • Zyvox®

Generic Available

No

Canadian Brand Names

  • Zyvoxam®

Pharmacologic Category

  • Antibiotic, Oxazolidinone

Pharmacologic Category Synonyms

  • Oxazolidinone Antibiotic

Use: Labeled Indications

Treatment of vancomycin-resistant Enterococcus faecium (VRE) infections, nosocomial pneumonia caused by Staphylococcus aureus including MRSA or Streptococcus pneumoniae (including multidrug-resistant strains [MDRSP]), complicated and uncomplicated skin and skin structure infections (including diabetic foot infections without concomitant osteomyelitis), and community-acquired pneumonia caused by susceptible gram-positive organisms

Pregnancy Risk Factor

C

Pregnancy Considerations

Because adverse effects were observed in some animal studies, linezolid is classified pregnancy category C. There are no adequate and well-controlled studies in pregnant women.

Lactation

Excretion in breast milk unknown/use caution

Breast-Feeding Considerations

It is not known if linezolid is excreted in human milk. Linezolid has low protein binding and is 100% bioavailable orally which may increase the exposure to a nursing infant. The manufacturer advises caution if administering linezolid to a breast-feeding woman. Linezolid is used therapeutically in infants. Nondose-related effects could include modification of bowel flora.

Contraindications

Hypersensitivity to linezolid or any other component of the formulation; concurrent use or within 2 weeks of MAO inhibitors; patients with uncontrolled hypertension, pheochromocytoma, thyrotoxicosis, and/or taking sympathomimetics (eg, pseudoephedrine), vasopressive agents (eg, epinephrine, norepinephrine), or dopaminergic agents (eg, dopamine, dobutamine) unless closely monitored for increased blood pressure; patients with carcinoid syndrome and/or taking SSRIs, tricyclic antidepressants, serotonin 5-HT1B,1D receptor agonists, meperidine, or buspirone unless closely monitored for sign/symptoms of serotonin syndrome

Warnings/Precautions

Concerns related to adverse effects:

• Lactic acidosis: Has been reported with use. Patients who develop recurrent nausea and vomiting, unexplained acidosis, or low bicarbonate levels need immediate evaluation.

• Myelosuppression: Has been reported and may be dependent on duration of therapy (generally >2 weeks of treatment); use with caution in patients with pre-existing myelosuppression, in patients receiving other drugs which may cause bone marrow suppression, or in chronic infection (previous or concurrent antibiotic therapy). Weekly CBC monitoring is recommended; discontinue therapy in patients developing myelosuppression (or in whom myelosuppression worsens during treatment).

• Peripheral and optic neuropathy (with vision loss): Has been reported and may occur primarily with extended courses of therapy >28 days; any symptoms of visual change or impairment warrant immediate ophthalmic evaluation and possible discontinuation of therapy.

• Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.

Disease-related concerns:

• Carcinoid syndrome: Use with caution and closely monitor for serotonin syndrome in patients with carcinoid syndrome; linezolid has not been studied in patients with this condition. Use is contraindicated in the absence of close monitoring.

• Hypertension: Use with caution and closely monitor blood pressure in patients with uncontrolled hypertension; linezolid has not been studied in patients with this condition. Use is contraindicated in the absence of close monitoring.

• Hyperthyroidism: Use with caution and closely monitor blood pressure in patients with untreated hyperthyroidism; linezolid has not been studied in patients with this condition. Use is contraindicated in the absence of close monitoring.

• Pheochromocytoma: Use with caution and closely monitor blood pressure in patients with pheochromocytoma; linezolid has not been studied in patients with this condition. Use is contraindicated in the absence of close monitoring.

• Seizure disorder: Seizures have been reported; use with caution in patients with a history of seizures.

Concurrent drug therapy issues:

• Serotonin syndrome: Symptoms of agitation, confusion, hallucinations, hyper-reflexia, myoclonus, shivering, and tachycardia may occur with concomitant proserotonergic drugs (eg, SSRIs/SNRIs or triptans) or agents which reduce linezolid's metabolism; concurrent use with these medications is contraindicated unless patient is closely monitored for signs/symptoms of serotonin syndrome.

Special populations:

• Pediatrics: The manufacturer states that empiric use in pediatric patients with CNS infections is not recommended due to inconsistent concentrations in the CSF; however, there are multiple case reports describing successful treatment of documented VRE and Staphylococcus aureus CNS and shunt infections in the literature.

Dosage form specific issues:

• Phenylalanine: Oral suspension contains phenylalanine.

Other warnings/precautions:

• Appropriate use: Unnecessary use may lead to the development of resistance to linezolid; consider alternatives before initiating outpatient treatment.

• MAO inhibitor properties: Exhibits mild MAO inhibitor properties and has the potential to have the same interactions as other MAO inhibitors.

Adverse Reactions

Percentages as reported in adults; frequency similar in pediatric patients

>10%:

Central nervous system: Headache (<1% to 11%)

Gastrointestinal: Diarrhea (3% to 11%)

1% to 10%:

Central nervous system: Insomnia (3%), dizziness (?2%), fever (2%)

Dermatologic: Rash (2%)

Gastrointestinal: Nausea (3% to 10%), vomiting (1% to 4%), pancreatic enzymes increased (?4%), constipation (2%), taste alteration (1% to 2%), tongue discoloration (?1%), oral moniliasis (?1%), pancreatitis

Genitourinary: Vaginal moniliasis (1% to 2%)

Hematologic: Hemoglobin decreased (1% to 7%), thrombocytopenia (?3%), anemia, leukopenia, neutropenia; Note: Myelosuppression (including anemia, leukopenia, pancytopenia, and thrombocytopenia; may be more common in patients receiving linezolid for >2 weeks)

Hepatic: Abnormal LFTs (?10%), bilirubin increased (?1%)

Renal: BUN increased (?2%)

Miscellaneous: Fungal infection (0.1% to 2%), lactate dehydrogenase increased (<1% to 2%)

<1% or frequency not defined: Blurred vision, C. difficile-related complications, creatinine increased, dyspepsia, hypertension, localized abdominal pain, pruritus

Postmarketing and/or case reports: Anaphylaxis, angioedema, bullous skin disorders, lactic acidosis, peripheral neuropathy, optic neuropathy, seizures, serotonin syndrome (with concurrent use of other serotonergic agents), Stevens-Johnson syndrome, vision loss

Drug Interactions

Alpha-/Beta-Agonists (Direct-Acting): MAO Inhibitors may enhance the vasopressor effect of Alpha-/Beta-Agonists (Direct-Acting). Primarily with oral administration of phenylephrine. Exceptions: Dipivefrin. Risk D: Consider therapy modification

Alpha-/Beta-Agonists (Indirect-Acting): MAO Inhibitors may enhance the hypertensive effect of Alpha-/Beta-Agonists (Indirect-Acting). Risk X: Avoid combination

Alpha1-Agonists: MAO Inhibitors may enhance the hypertensive effect of Alpha1-Agonists. Risk X: Avoid combination

Alpha2-Agonists (Ophthalmic): MAO Inhibitors may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). Risk X: Avoid combination

Altretamine: May enhance the orthostatic effect of MAO Inhibitors. Risk C: Monitor therapy

Amphetamines: MAO Inhibitors may enhance the hypertensive effect of Amphetamines. Risk X: Avoid combination

Anilidopiperidine Opioids: May enhance the serotonergic effect of MAO Inhibitors. This could result in serotonin syndrome. Management: Avoid use of fentanyl (and other anilidopiperidine opioids when possible) in patients who have used a monoamine oxidase inhibitor within the past 14 days due to reports of unpredictable but severe adverse effects. Risk X: Avoid combination

Antihypertensives: MAO Inhibitors may enhance the hypotensive effect of Antihypertensives. MAO Inhibitors may enhance the orthostatic effect of Antihypertensives. Risk C: Monitor therapy

Atomoxetine: MAO Inhibitors may enhance the neurotoxic (central) effect of Atomoxetine. Risk X: Avoid combination

Beta2-Agonists: MAO Inhibitors may enhance the adverse/toxic effect of Beta2-Agonists. Risk C: Monitor therapy

BuPROPion: MAO Inhibitors may enhance the neurotoxic (central) effect of BuPROPion. Risk X: Avoid combination

BusPIRone: May enhance the adverse/toxic effect of MAO Inhibitors. Elevated blood pressure has been reported. Risk X: Avoid combination

CarBAMazepine: May enhance the adverse/toxic effect of MAO Inhibitors. Risk X: Avoid combination

COMT Inhibitors: May enhance the adverse/toxic effect of MAO Inhibitors. Risk D: Consider therapy modification

Cyclobenzaprine: May enhance the serotonergic effect of MAO Inhibitors. This could result in serotonin syndrome. Risk X: Avoid combination

Dexmethylphenidate: MAO Inhibitors may enhance the hypertensive effect of Dexmethylphenidate. Risk X: Avoid combination

Dextromethorphan: MAO Inhibitors may enhance the serotonergic effect of Dextromethorphan. This may cause serotonin syndrome. Risk X: Avoid combination

Levodopa: May enhance the adverse/toxic effect of MAO Inhibitors. Of particular concern is the development of hypertensive reactions when levodopa is used with nonselective MAOI. Risk D: Consider therapy modification

Lithium: MAO Inhibitors may enhance the adverse/toxic effect of Lithium. Risk C: Monitor therapy

MAO Inhibitors: May enhance the adverse/toxic effect of Linezolid. Risk X: Avoid combination

Maprotiline: May enhance the adverse/toxic effect of MAO Inhibitors. Risk X: Avoid combination

Meperidine: MAO Inhibitors may enhance the serotonergic effect of Meperidine. This may cause serotonin syndrome. Risk X: Avoid combination

Methyldopa: MAO Inhibitors may enhance the adverse/toxic effect of Methyldopa. Risk X: Avoid combination

Methylphenidate: MAO Inhibitors may enhance the hypertensive effect of Methylphenidate. Risk X: Avoid combination

Mirtazapine: MAO Inhibitors may enhance the neurotoxic (central) effect of Mirtazapine. Risk X: Avoid combination

Orthostasis Producing Agents: MAO Inhibitors may enhance the orthostatic effect of Orthostasis Producing Agents. Risk C: Monitor therapy

Propoxyphene: May enhance the adverse/toxic effect of MAO Inhibitors. Specifically, the risk of serotonin syndrome or other serotonergic adverse events may be increased. Risk X: Avoid combination

Rauwolfia Alkaloids: MAO Inhibitors may enhance the adverse/toxic effect of Rauwolfia Alkaloids. Existing MAOI therapy can result in paradoxical effects of added rauwolfia alkaloids (eg, excitation, hypertension). Risk D: Consider therapy modification

Selective Serotonin Reuptake Inhibitors: MAO Inhibitors may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Risk X: Avoid combination

Serotonin 5-HT1D Receptor Agonists: MAO Inhibitors may decrease the metabolism of Serotonin 5-HT1D Receptor Agonists. Management: If MAO inhibitor therapy is required, naratriptan, eletriptan or frovatriptan may be a suitable 5-HT1D agonist to employ. Exceptions: Eletriptan; Frovatriptan; Naratriptan. Risk X: Avoid combination

Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Risk D: Consider therapy modification

Serotonin/Norepinephrine Reuptake Inhibitors: MAO Inhibitors may enhance the serotonergic effect of Serotonin/Norepinephrine Reuptake Inhibitors. This may cause serotonin syndrome. Risk X: Avoid combination

Sibutramine: May enhance the serotonergic effect of Serotonin Modulators. This may cause serotonin syndrome. Risk X: Avoid combination

Tapentadol: May enhance the adverse/toxic effect of MAO Inhibitors. Risk X: Avoid combination

Tetrabenazine: May enhance the adverse/toxic effect of MAO Inhibitors. Risk X: Avoid combination

TraMADol: May enhance the neuroexcitatory and/or seizure-potentiating effect of MAO Inhibitors. Risk D: Consider therapy modification

Tricyclic Antidepressants: MAO Inhibitors may enhance the serotonergic effect of Tricyclic Antidepressants. This may cause serotonin syndrome. Risk X: Avoid combination

Ethanol/Nutrition/Herb Interactions

Ethanol: Avoid ethanol (based on CNS depressant effects and potential tyramine content)

Food: Concurrent ingestion of foods rich in tyramine may cause sudden and severe high blood pressure (hypertensive crisis). Avoid tyramine-containing foods with MAO-Is. Food's freshness is also an important concern; improperly stored or spoiled food can create an environment where tyramine concentrations may increase.

Herb/Nutraceutical: Avoid supplements containing caffeine, tyrosine, tryptophan or phenylalanine. Ingestion of large quantities may increase the risk of severe side effects (eg, hypertensive reactions, serotonin syndrome).

Storage

Infusion: Store at 25°C (77°F). Protect from light. Keep infusion bags in overwrap until ready for use. Protect infusion bags from freezing.

Oral suspension: Following reconstitution, store at 25°C (77°F). Use reconstituted suspension within 21 days. Protect from light.

Tablet: Store at 25°C (77°F). Protect from light; protect from moisture.

Reconstitution

Oral suspension: Reconstitute with 123 mL of distilled water (in 2 portions); shake vigorously. Concentration is 100 mg/5 mL. Prior to administration mix gently by inverting bottle; do not shake.

Compatibility

Stable in D5W, LR, NS

Y-site administration: Compatible: Acyclovir, alfentanil, amikacin, aminophylline, ampicillin, ampicillin sulbactam, aztreonam, bretylium, buprenorphine, butorphanol, calcium gluconate, carboplatin, cefazolin, cefotetan, cefoxitin, ceftazidime, ceftizoxime, ceftriaxone, cefuroxime, cimetidine, ciprofloxacin, cisatracurium, cisplatin, clindamycin, cyclophosphamide, cyclosporine, cytarabine, dexamethasone, dexmedetomidine, D51/2 NS, D5NS, digoxin, diphenhydramine, dobutamine, dopamine, doxorubicin, doxycycline, droperidol, enalaprilat, Esmolol, etoposide phosphate, famotidine, fenoldopam, fentanyl, fluconazole, fluorouracil, furosemide, ganciclovir, gemcitabine, gentamicin, granisetron, haloperidol, heparin, hydrocortisone sodium succinate, hydromorphone, hydroxyzine, ifosfamide, imipenem, labetalol, leucovorin, levofloxacin, lidocaine, lorazepam, magnesium sulfate, mannitol, ,meperidine, meropenem, mesna, methotrexate, methylprednisolone sodium succinate, metoclopramide, metronidazole, midazolam, mitoxantrone, morphine, nalbuphine, naloxone, nicardipine, nitroglycerin, ofloxacin, ondansetron, paclitaxel, pentobarbital, phenobarbital, piperacillin (tazobactam), potassium chloride, prochlorperazine, promethazine, propranolol, ranitidine remifentanil, sodium bicarbonate, sufentanil, theophylline, tobramycin, vancomycin, vecuronium, verapamil, vincristine, zidovudine. Incompatible: Amphotericin B, chlorpromazine, diazepam, erythromycin, pentamidine, phenytoin, sulfamethoxazole/trimethoprim.

Compatibility when admixed: Compatible: Aztreonam, cefazolin, ceftazidime, ciprofloxacin, gentamicin, levofloxacin, ofloxacin, tobramycin. Incompatible: Ceftriaxone, erythromycin, sulfamethoxazole/trimethoprim.

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: Vdss: Adults: 40-50 L

Protein binding: Adults: 31%

Metabolism: Hepatic via oxidation of the morpholine ring, resulting in two inactive metabolites (aminoethoxyacetic acid, hydroxyethyl glycine); does not involve CYP

Bioavailability: Oral: ~100%

Half-life elimination: Children ?1 week (full-term) to 11 years: 1.5-3 hours; Adults: 4-5 hours

Time to peak: Adults: Oral: 1-2 hours

Excretion: Urine (30% as parent drug, 50% as metabolites); feces (9% as metabolites)

Nonrenal clearance: ~65%; increased in children ?1 week to 11 years

Dosage

Oral, I.V.:

VRE infections including concurrent bacteremia:

Preterm neonates (<34 weeks gestational age): 10 mg/kg every 12 hours; neonates with a suboptimal clinical response can be advanced to 10 mg/kg every 8 hours. By day 7 of life, all neonates should receive 10 mg/kg every 8 hours.

Infants (excluding preterm neonates <1 week) and Children ?11 years: 10 mg/kg every 8 hours for 14-28 days

Children ?12 years and Adults: 600 mg every 12 hours for 14-28 days

MRSA: Adults: 600 mg every 12 hours

Nosocomial pneumonia, complicated skin and skin structure infections, community acquired pneumonia including concurrent bacteremia: Oral, I.V.:

Preterm neonates (<34 weeks gestational age): 10 mg/kg every 12 hours; neonates with a suboptimal clinical response can be advanced to 10 mg/kg every 8 hours. By day 7 of life, all neonates should receive 10 mg/kg every 8 hours.

Infants (excluding preterm neonates <1 week) and Children ?11 years: 10 mg/kg every 8 hours for 10-14 days

Children ?12 years and Adults: 600 mg every 12 hours for 10-14 days

Uncomplicated skin and skin structure infections: Oral:

Preterm neonates (<34 weeks gestational age): 10 mg/kg every 12 hours; neonates with a suboptimal clinical response can be advanced to 10 mg/kg every 8 hours. By day 7 of life, all neonates should receive 10 mg/kg every 8 hours.

Infants (excluding preterm neonates <1 week) and Children <5 years: 10 mg/kg every 8 hours for 10-14 days

Children 5-11 years: 10 mg/kg every 12 hours for 10-14 days

Children ?12-18 years: 600 mg every 12 hours for 10-14 days

Adults: 400 mg every 12 hours for 10-14 days

Note: 400 mg dose is recommended in the product labeling; however, 600 mg dose is commonly employed clinically

Elderly: No dosage adjustment required

Dosage adjustment in renal impairment: No adjustment is 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. Monitor for hematopoietic (eg, anemia, leukopenia, thrombocytopenia) and neuropathic (eg, peripheral neuropathy) adverse events when administering for extended periods. Both linezolid and the two metabolites are eliminated by dialysis. Linezolid should be given after hemodialysis.

Continuous renal replacement therapy (CRRT): No adjustment needed.

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.

Administration: Oral

Oral suspension: Invert gently to mix prior to administration, do not shake. Administer without regard to meals.

Administration: I.V.

Administer intravenous infusion over 30-120 minutes. Do not mix or infuse with other medications. When the same intravenous line is used for sequential infusion of other medications, flush line with D5W, NS, or LR before and after infusing linezolid. The yellow color of the injection may intensify over time without affecting potency.

Monitoring Parameters

Weekly CBC and platelet counts, particularly in patients at increased risk of bleeding, with pre-existing myelosuppression, on concomitant medications that cause bone marrow suppression, in those who require >2 weeks of therapy, or in those with chronic infection who have received previous or concomitant antibiotic therapy; visual function with extended therapy (?3 months) or in patients with new onset visual symptoms, regardless of therapy length

Dietary Considerations

Take without regard to meals. Avoid consuming large amounts of tyramine-containing foods/beverages. Some examples include aged or matured cheese, air-dried or cured meats (including sausages and salamis), fava or broad bean pods, tap/draft beers, Marmite concentrate, sauerkraut, soy sauce and other soybean condiments.

Some products may contain phenylalanine.

Patient Education

Oral: Take exactly as directed. Suspension; store at room temperature and use within 21 days. Do not alter dosage without consulting prescriber. Complete full course of therapy even if condition appears controlled. Maintain adequate hydration unless instructed to restrict fluid intake. Avoid alcohol. Avoid tyramine-containing foods (eg, pickles, aged cheese, wine).

Oral/I.V.: You may experience mild headache (analgesic may help); GI discomfort, nausea, vomiting, taste alteration (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help); or constipation (increase exercise, fluids, fruit, or fiber may help). Report immediately unresolved, white plaques in mouth; skin rash or irritation; acute headache, dizziness, blurred vision, or changes in visual acuity; tingling or numbness in extremities; persistent diarrhea; or other persistent adverse reactions. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.

Geriatric Considerations

According to the manufacturer the pharmacokinetics of linezolid are not significantly altered in persons ?65 years of age.

Anesthesia and Critical Care Concerns/Other Considerations

Clinical Pearls/Comments: Linezolid has mild MAO inhibitor properties and should be used with caution in patients with cardiovascular disease, particularly those with hypertension. Avoid use with sympathomimetic and dopaminergic agents (serotonin reuptake inhibitors, tricyclic antidepressants, serotonin 5-HT1 receptor agonists, meperidine, or buspirone).

Linezolid has time-dependent kill characteristics; time for which the serum concentration remains above the MIC for a dosing period is the best predictor of efficacy. With prolonged exposure (>2 weeks), monitor closely for anemia, leukopenia, and thrombocytopenia.

Evidence-Based Information:

Trial Showing Increased Rate of Death in Catheter-Related Bloodstream Infections - March, 2007: The U.S. Food and Drug Administration (FDA) has issued an alert to healthcare professionals regarding an increased rate of death among patients treated with linezolid (Zyvox®) for catheter-related bacteremia and catheter-site infections. Healthcare professionals are reminded that linezolid is not approved for the treatment of catheter-related bloodstream, catheter-site, or gram-negative infections. Additional information is available at http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm152993.htm

Cardiovascular Considerations

Linezolid has mild MAO inhibitor properties and should be used with caution in patients with cardiovascular disease, particularly those with hypertension. Avoid use with sympathomimetic and dopaminergic agents. Linezolid can cause thrombocytopenia. Use cautiously in patients with thrombocytopenia, or in patients being started on medications that can cause thrombocytopenia (eg, heparin).

Dental Health: Effects on Dental Treatment

Key adverse event(s) related to dental treatment: Oral moniliasis, taste alteration, and tongue discoloration.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

Linezolid has mild monoamine oxidase inhibitor properties. The clinician is reminded that vasoconstrictors have the potential to interact with MAO-Is to result in elevation of blood pressure. Caution is suggested.

Mental Health: Effects on Mental Status

May cause insomnia and dizziness

Mental Health: Effects on Psychiatric Treatment

Has mild MAO inhibitor properties and has the potential to have the same interactions as other MAO inhibitors; thrombocytopenia has been reported and may be dependent on duration of therapy (generally >2 weeks of treatment), caution with valproic acid; avoid use with serotonergic agents such as TCAs, venlafaxine, trazodone, sibutramine, meperidine, dextromethorphan, and SSRIs; may cause leukopenia, use caution with clozapine and carbamazepine

Nursing: Physical Assessment/Monitoring

Assess for previous drug allergies before administering first dose. Assess other pharmacological agents patient may be taking for effectiveness and interactions (eg, serotonergic agents may increase resistance to linezolid and increase risk of serotonin syndrome, hypertension with adrenergic agents, or myelosuppression with other drugs that may cause bone marrow suppression). Assess results of laboratory tests (weekly CBC and platelet count), therapeutic effectiveness (resolution of infection), and adverse reactions (eg, myelosuppression [anemia, leukopenia, pancytopenia, and thrombocytopenia; may be more common in patients receiving linezolid for >2 weeks], lactic acidosis; peripheral or optic neuropathy) on a regular basis. Teach patient proper use (oral), possible side effects/appropriate interventions (eg, tyramine-free diet; see Tyramine Contents of Foods list), and adverse symptoms to report.

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Infusion [premixed]:

Zyvox®: 200 mg (100 mL) [contains sodium 1.7 mEq]; 600 mg (300 mL) [contains sodium 5 mEq]

Powder for oral suspension:

Zyvox®: 20 mg/mL (150 mL) [contains phenylalanine 20 mg/5 mL, sodium benzoate, and sodium 0.4 mEq/5 mL; orange flavor]

Tablet:

Zyvox®: 600 mg [contains sodium 0.1 mEq/tablet]

Pricing: U.S. (www.drugstore.com)

Tablets (Zyvox)

600 mg (20): $1642.39

References

American Thoracic Society and Infectious Diseases Society of America, “Guidelines for the Management of Adults With Hospital-Acquired, Ventilator-Associated, and Healthcare-Associated Pneumonia,” Am J Respir Crit Care Med, 2005, 171(4):388-416.

Bain KT and Wittbrodt ET, “Linezolid for the Treatment of Resistant Gram-Positive Cocci,” Ann Pharmacother, 2001, 35(5):566-75.

Cook AM, Ramsey CN, Martin CA, et al, “Linezolid for the Treatment of a Heteroresistant Staphylococcus aureus Shunt Infection,” Pediatr Neurosurg, 2005, 41(2):102-4.

da Silva PS, Monteiro Neto H, and Sejas LM, “Successful Treatment of Vancomycin-Resistant Enterococcus Ventriculitis in a Child,” Braz J Infect Dis, 2007, 11(2):297-9.

Mandell LA, Wunderink RG, Anzueto A, et al, "Infectious Diseases Society of America/American Thoracic Society Consensus Guidelines on the Management of Community-Acquired Pneumonia in Adults," Clin Infect Dis, 2007, 44(Suppl 2):27-72.

Milstone AM, Dick J, Carcon B, et al, “Cerebrospinal Fluid Penetration and Bacteriostatic Activity of Linezolid Against Enterococcus faecalis in a Child With a Ventriculoperitoneal Shunt Infection,” Pediatr Neurosurg, 2007, 43(5):406-9.

Perry CM and Jarvis B, “Linezolid: A Review of Its Use in the Management of Serious Gram-Positive Infections,” Drugs, 2001, 61(4):525-51.

Roberts JA and Lipman J, "Antibacterial Dosing in Intensive Care: Pharmacokinetics, Degree of Disease and Pharmacodynamics of Sepsis," Clin Pharmacokinet, 2006, 45(8):755-73.

Shaikh ZH, Peloquin CA, and Ericsson CD, “Successful Treatment of Vancomycin-Resistant Enterococcus faecium Meningitis With Linezolid: Case Report and Literature Review,” Scand J Infect Dis, 2001, 33(5):375-9.

Shulman KI and Walker SE, “A Reevaluation of Dietary Restrictions for Irreversible Monoamine Oxidase Inhibitors,” Psychiatr Ann, 2001, 31(6):378-84.

Shulman KI and Walker SE, “Refining the MAOI Diet: Tyramine Content of Pizzas and Soy Products,” J Clin Psychiatry, 1999, 60(3):191-3.

Trotman RL, Williamson JC, Shoemaker DM, et al, "Antibiotic Dosing in Critically Ill Adult Patients Receiving Continuous Renal Replacement Therapy," Clin Infect Dis, 2005, 41(8):1159-66.

Walker SE, Shulman KI, Tailor SA, et al, “Tyramine Content of Previously Restricted Foods in Monoamine Oxidase Inhibitor Diets,” J Clin Psychopharmacol, 1996, 16(5):383-8.

Villani P, Regazzi MB, Marubbi F, et al, “Cerebrospinal Fluid Linezolid Concentrations in Postneurosurgical Central Nervous System Infections,” Antimicrob Agents Chemother, 2002, 46(3):936-7.

International Brand Names

  • Linox (IN)
  • Zyvox (AE, AR, AU, BH, BR, CL, CN, CR, CY, EC, EG, GB, GT, HK, HN, ID, IE, IL, IQ, IR, JO, KP, KW, LB, LY, MY, NI, OM, PA, PE, PH, QA, SA, SG, SV, SY, TH, UY, VE, YE)
  • Zyvoxam (MX)
  • Zyvoxid (BE, CH, CO, CZ, DE, DK, EE, FI, FR, HN, IL, IT, NL, NO, PL, SE, ZA)

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Last full review/revision October 2009