Zyvox: Targeted Gram-Positive Infection Treatment
| Product dosage: 600mg | |||
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Synonyms | |||
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 option in the antimicrobial arsenal, particularly against 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, distinguishing it from other antibiotic classes and reducing the potential for cross-resistance. This profile provides a comprehensive overview for healthcare professionals considering its use in complex clinical scenarios.
Features
- Active Ingredient: Linezolid
- Available Formulations: Film-coated tablets (600 mg), oral suspension (100 mg/5 mL), 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: Gram-positive bacteria including Staphylococcus aureus (methicillin-susceptible and -resistant strains), Streptococcus pneumoniae (including multidrug-resistant strains), and Enterococcus faecium (vancomycin-resistant strains)
- Bioavailability: Approximately 100% following oral administration, permitting seamless transition from IV to oral therapy
Benefits
- Provides potent bactericidal activity against resistant Gram-positive organisms where treatment options may be limited
- Offers excellent oral bioavailability, facilitating early discharge and outpatient parenteral antibiotic therapy (OPAT) transitions, reducing hospital stays and associated costs
- Demonstrates a unique mechanism of action, minimizing cross-resistance with other antibiotic classes such as beta-lactams, glycopeptides, and macrolides
- Effective in treating complicated skin and skin structure infections, hospital-acquired and community-acquired pneumonia, and vancomycin-resistant Enterococcus faecium infections
- Supported by robust clinical trial data showing non-inferiority to vancomycin and other comparators in approved indications
- Available in multiple formulations (tablet, suspension, IV) to accommodate various patient populations and clinical settings
Common use
Zyvox is indicated for the treatment of adults and specific pediatric populations with infections caused by susceptible strains of designated Gram-positive microorganisms. Approved indications include complicated skin and skin structure infections (including diabetic foot infections without concomitant osteomyelitis), hospital-acquired pneumonia known or suspected to be caused by MRSA, community-acquired pneumonia caused by Streptococcus pneumoniae (including multidrug-resistant strains), and vancomycin-resistant Enterococcus faecium infections. Its use is generally reserved for situations where resistance to other agents is confirmed or strongly suspected, or in cases of beta-lactam hypersensitivity, aligning with antimicrobial stewardship principles to preserve efficacy.
Dosage and direction
The recommended dosage for most adult indications is 600 mg administered intravenously or orally every 12 hours. Treatment duration typically ranges from 10 to 14 days, though longer courses may be required for specific infections such as osteomyelitis (off-label use requires careful benefit-risk assessment). No dosage adjustment is necessary when switching between intravenous and oral administration. For pediatric patients, dosing is weight-based: 10 mg/kg every 8 hours for children under 12 years (not exceeding 600 mg/dose). Oral suspension should be shaken gently before administration. Zyvox may be taken with or without food.
Precautions
Myelosuppression (including anemia, leukopenia, pancytopenia, and thrombocytopenia) has been reported; complete blood counts should be monitored weekly, especially in patients receiving therapy longer than 2 weeks, those with pre-existing myelosuppression, or those receiving concomitant medications that may cause bone marrow suppression. Peripheral and optic neuropathy (sometimes progressing to vision loss) has been reported, primarily with prolonged use (>28 days); patients should be monitored for visual function and advised to report any symptoms of neuropathy. Serotonin syndrome has occurred in patients taking Zyvox concomitantly with serotonergic drugs; monitor for mental status changes, autonomic instability, and neuromuscular abnormalities. Lactic acidosis has been reported; evaluate any unexplained metabolic acidosis. Use with caution in patients with uncontrolled hypertension, pheochromocytoma, carcinoid syndrome, or untreated hyperthyroidism.
Contraindications
Zyvox is contraindicated in patients with known hypersensitivity to linezolid or any other component of the formulation. It should not be used in patients taking, or within two weeks of taking, monoamine oxidase inhibitors (MAOIs) or other agents with significant MAOI activity (e.g., phenelzine, isocarboxazid) due to the risk of severe pressor response. Avoid use in patients with uncontrolled hypertension, pheochromocytoma, thyrotoxicosis, and/or those taking sympathomimetic agents (e.g., pseudoephedrine), vasopressive agents (e.g., epinephrine, norepinephrine), or dopaminergic agents. Contraindicated in patients with carcinoid syndrome due to theoretical risk of serotonin syndrome.
Possible side effect
Common adverse reactions (≥5% incidence) include diarrhea, headache, nausea, and vomiting. Hematologic effects such as thrombocytopenia and anemia may occur, particularly with prolonged therapy. Less frequently reported events include oral candidiasis, vaginal candidiasis, taste alteration, insomnia, dizziness, and elevated liver enzymes. Serious but rare adverse effects include peripheral neuropathy, optic neuropathy, serotonin syndrome, lactic acidosis, hypoglycemia, and Clostridioides difficile-associated diarrhea. Allergic reactions, including skin rashes and anaphylaxis, have been reported. Pseudomembranous colitis has been observed with nearly all antibacterial agents and may range in severity from mild to life-threatening.
Drug interaction
Zyvox exhibits weak, reversible nonselective inhibition of monoamine oxidase (MAO); therefore, concomitant administration with adrenergic and serotonergic agents requires caution. Avoid concomitant use with serotonergic psychiatric medications (SSRIs, SNRIs, TCAs, triptans, buspirone) due to increased risk of serotonin syndrome. Potent CYP450 inducers (e.g., rifampin, carbamazepine, phenytoin) may decrease linezolid plasma concentrations. Avoid use with large quantities of tyramine-rich foods (aged cheeses, fermented meats, draft beers, soy products) as hypertensive crisis may occur. May enhance the pressor response to sympathomimetic agents like pseudoephedrine or phenylpropanolamine. Use caution with drugs that affect platelet function (e.g., NSAIDs, SSRIs) due to potential additive effects on bleeding risk.
Missed dose
If a dose is missed, it should be taken as soon as possible. However, if it is almost time for the next scheduled dose, the missed dose should be skipped and the regular dosing schedule resumed. Doubling the dose to make up for a missed dose is not recommended. Patients should be advised to maintain the twice-daily (or, in pediatric cases, thrice-daily) dosing schedule as consistently as possible to maintain effective plasma concentrations and minimize the risk of resistance development.
Overdose
There is limited experience with Zyvox overdose. Reported cases have included episodes of serotonin syndrome requiring supportive care. There is no specific antidote for linezolid overdose. Management should include supportive care, maintaining glomerular filtration, and monitoring hematologic parameters and mental status. Hemodialysis may accelerate elimination, as approximately 30% of a dose is removed by dialysis; however, data are limited. Symptomatic treatment for serotonin syndrome (which may include benzodiazepines, cyproheptadine, and temperature control) may be necessary. Contact a poison control center for current guidance on management.
Storage
Store Zyvox tablets and oral suspension at controlled room temperature, 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C and 30°C (59°F and 86°F). Protect from light and moisture. Keep the bottle of oral suspension tightly closed. The reconstituted oral suspension may be stored at room temperature and should be used within 21 days. Do not freeze. Intravenous solutions should be protected from light and stored at room temperature. Keep out of reach of children and pets. Do not use beyond the expiration date printed on the packaging.
Disclaimer
This information is intended for healthcare professionals and is not a substitute for clinical judgment. Prescribers should consult full prescribing information and relevant clinical guidelines before initiating therapy. Dosage and administration must be individualized based on the patient’s clinical condition, renal/hepatic function, and microbiological findings. Use of antibacterial agents, including Zyvox, should be guided by susceptibility testing and local resistance patterns to preserve effectiveness and reduce the development of drug-resistant bacteria.
Reviews
Clinical studies and post-marketing surveillance demonstrate that Zyvox is an effective option for resistant Gram-positive infections, with high clinical cure rates in approved indications. Many infectious disease specialists value its oral bioavailability and unique mechanism, though note the need for vigilance regarding hematologic and neurologic adverse effects with prolonged courses. Its role is well-established within antimicrobial stewardship programs as a targeted agent for specific resistant pathogens. Long-term real-world evidence supports its efficacy but underscores the importance of appropriate patient selection and monitoring to mitigate risks.