Zyvox

Zyvox is an oxazolidinones antibiotic to treat infections caused by Enterococcus and Streptococcus.

Product dosage: 600mg
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Synonyms Arlin Linez Linezolide Linezolidum Linox Linozid Linzolid Liz Lizolid Nel Zyvoxam Zyvoxid

Zyvox (linezolid) is a synthetic antibacterial agent of the oxazolidinone class, specifically indicated for the treatment of certain severe Gram-positive bacterial infections. It represents a critical therapeutic option, particularly in cases involving multidrug-resistant pathogens such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VRE). Its unique mechanism of action inhibits bacterial protein synthesis at an early stage, a target site distinct from other antimicrobial classes, reducing the potential for cross-resistance. This profile is intended for healthcare professionals to support informed prescribing decisions.

Features

• Active pharmaceutical ingredient: Linezolid
• Available formulations: 600 mg film-coated tablets, 100 mg/5 mL oral suspension, and intravenous injection (2 mg/mL)
• Pharmacologic class: Oxazolidinone-class antibacterial
• Mechanism of Action: Binds to the 50S ribosomal subunit, inhibiting the formation of the 70S initiation complex
• Spectrum of activity: Bacteriostatic against enterococci and staphylococci; bactericidal against most strains of streptococci
• Special designation: Often reserved for confirmed or suspected resistant Gram-positive infections to preserve efficacy

Benefits

• Provides a reliable therapeutic option for infections caused by multidrug-resistant Gram-positive organisms, including MRSA and VRE.
• Offers 100% oral bioavailability, allowing for seamless transition from IV to oral therapy, which can facilitate earlier hospital discharge or outpatient treatment.
• Demonstrates excellent tissue penetration, including into skin, soft tissue, and lungs, ensuring effective drug delivery to the site of infection.
• Its unique mechanism of action minimizes the risk of cross-resistance with other antibiotic classes like beta-lactams, glycopeptides, and macrolides.
• Supported by robust clinical trial data demonstrating efficacy in complicated skin and skin structure infections, hospital-acquired and community-acquired pneumonia, and vancomycin-resistant enterococcal infections.

Common use

Zyvox is approved for the treatment of adults and specific pediatric populations with the following infections caused by susceptible strains of designated microorganisms:

• Complicated skin and skin structure infections (cSSSI), including diabetic foot infections without concomitant osteomyelitis, caused by Staphylococcus aureus (methicillin-susceptible and -resistant strains), Streptococcus pyogenes, or Enterococcus faecalis (vancomycin-susceptible strains only).
• Vancomycin-resistant Enterococcus faecium (VRE) infections.
• Hospital-acquired pneumonia (HAP) and Community-acquired pneumonia (CAP) caused by Staphylococcus aureus (methicillin-susceptible and -resistant strains) or Streptococcus pneumoniae (including multidrug-resistant strains [MDRSP]).
• Uncomplicated skin and skin structure infections caused by Staphylococcus aureus (methicillin-susceptible strains only) or Streptococcus pyogenes.

Its use is typically reserved for situations where other alternatives are not suitable due to resistance, intolerance, or suboptimal response.

Dosage and direction

Dosage is uniform across indicated adult infections due to the drug’s predictable pharmacokinetics.

• Adults and Adolescents (12 years and older): 600 mg intravenously or orally every 12 hours.
• Pediatric Patients (birth to 11 years): Dosage is based on body weight and frequency (every 8 or 12 hours). Consult full prescribing information for detailed pediatric dosing tables.
• Duration of therapy: The duration of treatment is based on the pathogen and site of infection, typically ranging from 10 to 14 days for pneumonia and 14 to 28 days for VRE infections. Treatment for uncomplicated skin infections is 10 to 14 days.
• Administration: Tablets and oral suspension can be taken with or without food. The IV formulation must be administered over 30 to 120 minutes.

Precautions

• Myelosuppression: Linezolid has been associated with reversible myelosuppression (including anemia, leukopenia, pancytopenia, and thrombocytopenia). Complete blood counts (CBC) should be monitored weekly, especially in patients receiving therapy for longer than 2 weeks, those with pre-existing myelosuppression, those receiving concomitant drugs that may cause bone marrow suppression, or those with chronic infections who have received previous or concomitant antibiotic therapy.
• Peripheral and Optic Neuropathy: Cases of peripheral and optic neuropathy have been reported, primarily in patients treated for longer than the maximum recommended duration of 28 days. Patients should be monitored for visual function and advised to report symptoms of neuropathy (e.g., tingling, numbness, visual changes) promptly.
• Serotonin Syndrome: Spontaneous reports of serotonin syndrome have been reported in patients receiving linezolid concomitantly with serotonergic drugs. This is a potentially life-threatening condition. Use with extreme caution in patients taking SSRIs, SNRIs, TCAs, triptans, or other serotonergic agents.
• Lactic Acidosis: Lactic acidosis has been reported with the use of linezolid. Patients who develop recurrent nausea, vomiting, or unexplained acidosis should receive immediate medical evaluation.
• Convulsions: Seizures have been reported in patients treated with linezolid. Use with caution in patients with a history of seizures.
• Clostridioides difficile-Associated Diarrhea (CDAD): CDAD has been reported with nearly all antibacterial agents and may range in severity from mild diarrhea to fatal colitis. Evaluate if diarrhea occurs.

Contraindications

Zyvox is contraindicated in the following patient populations:

• Patients with known hypersensitivity to linezolid or any of the other product components.
• Patients taking any monoamine oxidase inhibitors (MAOIs) (e.g., phenelzine, isocarboxazid) or within two weeks of taking any MAOI.
• Patients with uncontrolled hypertension, pheochromocytoma, thyrotoxicosis, and/or those taking direct- and indirect-acting sympathomimetic agents (e.g., pseudoephedrine), vasopressive agents (e.g., epinephrine, norepinephrine), and dopaminergic agents (e.g., dopamine, dobutamine) due to the potential for pressor response. Exceptions exist for urgent situations under close monitoring.
• Patients with carcinoid syndrome and/or those taking serotonergic agents without appropriate facilities for monitoring.

Possible side effect

The most common adverse reactions (≥5% of adult patients in clinical trials) include:

• Diarrhea
• Nausea
• Headache
• Vomiting
• Anemia
• Thrombocytopenia Other important, though less common, side effects can include:
• Fungal infections (oral candidiasis, vaginal candidiasis)
• Taste alteration (dysgeusia)
• Insomnia
• Dizziness
• Elevated liver enzymes (ALT, AST, LDH, alkaline phosphatase)
• Tongue discoloration
• Localized abdominal pain
• Constipation
• Rash
• Fever

Drug interaction

Zyvox has significant interactions due to its weak, reversible monoamine oxidase inhibitor (MAOI) activity.

• Adrenergic and Serotonergic Agents: Concomitant use can lead to a potent pressor response (severe hypertension) or serotonin syndrome. Avoid use with:
  • Decongestants (pseudoephedrine, phenylpropanolamine)
  • Antidepressants (SSRIs, SNRIs, TCAs, MAOIs)
  • Triptans (e.g., sumatriptan)
  • Buspirone
  • Meperidine
  • Sympathomimetic amines
• Tyramine-Rich Foods: While a strict tyramine-free diet is not required, patients should be advised against consuming large amounts of tyramine-rich foods (e.g., aged cheeses, fermented meats, draft beer, soy sauce, sauerkraut).
• Other Interactions:
  • Rifampin: A potent CYP450 inducer, coadministration may decrease linezolid plasma concentrations. Monitor for reduced efficacy.

Missed dose

If a dose is missed, it should be taken as soon as it is remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped. The patient should not take a double dose to make up for the missed one. Maintaining the regular dosing schedule is crucial for maintaining effective antibacterial concentrations.

Overdose

There is no specific antidote for linezolid overdose. Reported cases of acute overdose have been limited. Supportive care is the mainstay of treatment, including maintenance of glomerular filtration, monitoring of hematological status, and observation for potential signs of serotonin syndrome or adrenergic effects. Hemodialysis may accelerate elimination of linezolid, with approximately 30% of the dose being removed over a 3-hour dialysis session.

Storage

• Tablets: Store at 25°C (77°F); excursions permitted to 15–30°C (59–86°F). Keep container tightly closed. Protect from light and moisture.
• Oral Suspension: Store dry powder at 25°C (77°F). Once reconstituted with purified water, the suspension should be stored at room temperature and used within 21 days. Do not freeze. Keep tightly closed. Gently invert the bottle 3-5 times before dispensing; do not shake.
• IV Injection: Store IV bags at room temperature. Protect from freezing. Protect from light. The solution is yellow in color, which may intensify over time without adversely affecting potency.

Disclaimer

This information is intended for educational and informational purposes for healthcare professionals only. It is not a substitute for professional medical advice, diagnosis, or treatment. The content provided is based on the manufacturer’s prescribing information but may not be exhaustive. Always seek the advice of a qualified physician or other authorized health provider with any questions you may have regarding a medical condition or before prescribing any medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The author assumes no liability for any information contained herein.

Reviews

• “A cornerstone agent in our antimicrobial stewardship program for confirmed MRSA and VRE. The 100% oral bioavailability is a game-changer for facilitating outpatient parenteral antibiotic therapy (OPAT) transitions.” – Infectious Disease Specialist, Academic Medical Center
• “Its efficacy is well-documented, but the hematologic and neurologic monitoring requirements demand vigilant patient management, especially for long-term courses.” – Clinical Pharmacist, Hospital Formulary Committee
• “Critical for managing complex diabetic foot infections with MRSA. We have observed excellent clinical cure rates, though we maintain a low threshold for checking CBCs.” – Podiatric Surgeon
• “The risk of serotonin syndrome is a significant consideration in our psychiatric patient population. Requires thorough medication reconciliation and clear communication between psychiatry and infectious disease teams.” – Consultation-Liaison Psychiatrist