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linezolid (Rx)Brand and Other Names:Zyvox

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injectable solution

  • 2mg/mL (100mL, 300mL infusion bags)

oral suspension

  • 100mg/5mL

tablet

  • 600mg
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Vancomycin-Resistant Enterococcal Infections

600 mg PO/IV q12hr for 14-28 days

Complicated Skin & Skin Structure Infections

600 mg PO/IV q12hr for 10-14 days

Uncomplicated Skin & Skin Structure Infections

400-600 mg PO q12hr for 10-14 days

Community-Acquired Pneumonia (Including Concurrent Bacteremia)

600 mg PO/IV q12hr for 10-14 days

Nosocomial Pneumonia

600 mg PO/IV q12hr for 10-14 days

Methicillin-Resistant Staphylococcal Infections

600 mg PO/IV q12hr

Methicillin-Susceptible Staphylococcus Aureus

600 mg PO/IV q12hr for 10-14 days

Dosing Considerations

Monitor: CBC count qWeek

Dosage Forms & Strengths

injectable solution

  • 2mg/mL (100mL, 300mL infusion bags)

oral suspension

  • 100mg/5mL

tablet

  • 600mg
more...

Complicated Skin & Skin Structure Infections

<12 years: 10 mg/kg PO/IV q8hr for 10-14 days 

≥12 years: 600 mg PO/IV q12hr for 10-14 days

Uncomplicated Skin & Skin Structure Infections

<5 years: 10 mg/kg PO q8hr for 10-14 days 

5-12 years: 10 mg/kg PO q12hr for 10-14 days

>12 years: 600 mg PO q12hr for 10-14 days

Pneumonia

<12 years: 10 mg/kg PO/IV q8hr for 10-14 days 

≥12 years: 600 mg PO/IV q12hr for 10-14 days

Vancomycin-Resistant Enterococcal Infections

<12 years: 10 mg/kg PO/IV q8hr for 14-28 days 

≥12 years: 600 mg PO/IV q12hr for 14-28 days

Dosing Considerations

Monitor: CBC count qWeek

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Interactions

Interaction Checker

linezolid and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Pediatrics

            • Diarrhea (7.8-10.8%)

            1-10%

            Headache (5.7-8.8%)

            Diarrhea (8.2-8.3%)

            Nausea (5.1-6.6%)

            Vomiting (2-4.3%)

            Dizziness (1.8-2.6%)

            Rash (1.1-2.3%)

            Vaginal moniliasis (1.1-1.8%)

            Taste alteration (1-1.8%)

            Oral moniliasis (0.5-1.7%)

            Abnormal LFTs (0.4-1.6%)

            Fungal infection (0.3-1.5%)

            Localized abdominal pain (1.2-1.3%)

            Tongue discoloration (0.3-1.3%)

            Generalized abdominal pain (0.9-1.2%)

            Pediatrics

            • Vomiting (2.9-9.4%)
            • Headache (0.9-6.5%)
            • Anemia (5.6%)
            • Thrombocytopenia (4.7%)
            • Nausea (1.9-3.7%)
            • Generalized abdominal pain (0.9-2.4%)
            • Localized abdominal pain (0.5-2.4%)
            • Loose stools (1.6-2.3%)
            • Eosinophilia (0.4-1.9%)
            • Pruritus, other than application site (0.8-1.4%)
            • Vertigo (1.2%)

            <1%

            Lactic acidosis

            Myelosuppression

            Peripheral neuropathy

            Disorder of optic nerve

            Serotonin syndrome

            Postmarketing Reports

            Superficial tooth discoloration

            Superficial tongue discoloration

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            Warnings

            Contraindications

            Hypersensitivity

            Within 14 days of taking MAO inhibitor

            Cautions

            Use caution in patients with pheochromocytoma, concurrent apraclonidine, brimonidine, uncontrolled hypertension, thyrotoxicosis, carcinoid syndrome, diabetes mellitus, or seizure disorders

            Use oral suspension with caution in phenylketonuria (contains phenylalanine)

            Not approved for gram-negative bacteria or for catheter-related infections; clinical study showed higher mortality rate with linezolid than with other antibiotics for these conditions

            Monitor for myelosuppression; consider discontinuation in patients who develop or have worsening myelosuppression

            Evaluate for clostridium difficile if diarrhea occurs

            Peripheral and optic neuropathy reported, especially in patients given extended courses of therapy >28 days

            May cause hypoglycemia; monitor blood glucose levels

            Lactic acidosis reported with use; immediately evaluate patients who develop recurrent unexplained acidosis with nausea and vomiting

            Superinfection may develop

            Serotonin syndrome

            • Avoid coadministration with serotonergic psychiatric drugs (eg, SSRIs, SNRIs, TCAs, MAOIs) unless indicated for life-threatening or urgent infections (eg, vancomycin-resistant enterococcal infections, nosocomial pneumonia, complicated skin and skin structure infections such as methicillin-resistant S aureus), due to increased risk of serotonin syndrome; linezolid may increase serotonin CNS levels by MAO-A inhibition
            • If linezolid must be administered to a patient currently taking a serotonergic drug, stop serotonergic drug immediately and monitor for CNS toxicity; serotonergic therapy may be resumed 24 hours after last linezolid dose or after 2 weeks of monitoring (5 weeks if fluoxetine was taken), whichever comes first; serotonergic psychiatric medications should be stopped at least 2 weeks in advance of linezolid therapy; fluoxetine should be stopped at least 5 weeks in advance due to longer half-life
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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Unknown; use caution

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Binds to bacterial 23S rRNA of the 50S subunit to prevent protein translation; also elicits nonselective MAO inhibition

            Absorption

            Rapid and extensive

            Bioavailability: 100%

            Peak plasma time: 1-2 hr

            Distribution

            Protein bound: 31%

            Vd: 40-50 L

            Metabolism

            Hepatic via oxidation of the morpholine ring, resulting in 2 inactive metabolites (aminoethoxyacetic acid, hydroxyethyl glycine); does not involve CYP

            Elimination

            Half-life: 4-5 hr (adults); 1.5-3hr

            Clearance: Nonrenal (65% of total clearance)

            Excretion: Urine (80% of administered dose [30% unchanged, 50% metabolites]); feces (9% [metabolites])

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            Administration

            IV Incompatibilities

            Additive: Kanamycin, phenytoin, ceftriaxone, erythromycin lactobionate, TMP-SMX

            Syringe: Ampicillin

            Y-site: Ampho B, chlorpromazine, diazepam, pentamidine, phenytoin

            IV Compatibilities

            Additive: Aztreonam, cefazolin, ceftazidime, ciprofloxacin, gentamicin, levofloxacin, ofloxacin, piperacillin, tobramycin

            Y-site: Acyclovir, alfentanil, amikacin, aminophylline, ampicillin, aztreonam, bretylium, buprenorphine, butorphanol, Ca-gluconate, cefazolin, cefoperazone, cefotetan, cefoxitin, ceftazidime, ceftizoxime, ceftriaxone, cefuroxime, cimetidine, ciprofloxacin, cisatracurium, cisplatin, clindamycin, cyclophosphamide, cyclosporine, cytarabine, dexamethasone Na-phosphate, dexmetedomidine, digoxin, diphenhydramine, dobutamine, dopamine, doxorubicin, doxycycline, droperidol, enalaprilat, esmolol, etoposide PO4, famotidine, fenoldopam, fluconazole, fluorouracil, furosemide, ganciclovir, gemcitabine, gentamycin, granisetron, haloperidol, heparin, hydrocortisone sodium succinate, hydromorphone, hydroxyzine, ifosfamide, imipenem-cilastatin, labetalol, leucovorin, lidocaine, lorazepam, magnesium sulfate, mannitol, meperidine, meropenem, mesna, methotrexate, methylprednisolone, metoclopramide, metronidazole, midazolam, minocycline, mitoxantrone, morphine sulfate, nalbuphine, nicardipine, naloxone, nitroglycerin, ofloxacin, ondansetron, paclitaxel, pentobarbital, piperacillin, KCl, prochlorperazine, promethazine, propranolol, ranitidine, remifentanil, Na-bicarbonate, sufentanil, theophylline, ticarcillin, tobramycin, vancomycin, vecuronium, verapamil, vincristine, zidovudine

            IV Preparation

            Injection is supplied as a single-use, ready-to-use infusion bag; inspect for particulate matter and minute leaks in bag

            Infusion should be administered over 30-120 min

            Use reconstituted suspension within 21 days

            Storage

            Store at 25°C (77°F)

            Protect from light

            Keep infusion bags in overwrap until ready to use

            Protect infusion bags from freezing

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            Images

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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

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            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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