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Linezolid
Linezolid is a synthetic antibiotic belonging to the oxazolidinone class, used to treat serious bacterial infections caused by gram-positive bacteria. It is particularly effective against resistant strains such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). Linezolid is often reserved for infections that do not respond to other antibiotics and is used to treat conditions such as pneumonia, skin and soft tissue infections, and bacteremia. It works by inhibiting bacterial protein synthesis, preventing the bacteria from multiplying and spreading.
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Frequently Asked Questions
How long does it take for Linezolid to start working?
Linezolid begins working against bacterial infections within 24 to 48 hours, but it may take several days for symptoms to improve. Complete the full course of therapy as prescribed, even if you feel better before finishing.
What should I do if I miss a dose of Linezolid?
If you miss a dose, take it as soon as you remember. If it’s almost time for your next dose, skip the missed dose and resume your regular schedule. Do not double up on doses.
Can I drink alcohol while taking Linezolid?
While alcohol does not directly interact with Linezolid, it is best to avoid alcohol, as it can increase the risk of side effects such as dizziness or gastrointestinal discomfort.
Is Linezolid safe for long-term use?
Linezolid is typically used for short-term treatment of infections. Long-term use (beyond 28 days) can increase the risk of serious side effects such as neuropathy and myelosuppression. Regular monitoring is required for extended treatment.
What foods should I avoid while taking Linezolid?
Avoid tyramine-rich foods such as aged cheeses, smoked meats, fermented foods, soy sauce, and red wine, as these can interact with Linezolid and cause hypertensive crises.
Comprehensive Drug Guide
How Does Linezolid Work?
Linezolid works by inhibiting the bacterial ribosome at the 50S subunit, a critical component in the production of proteins necessary for bacterial growth and reproduction. By preventing the formation of the 70S initiation complex that bacteria need to synthesize proteins, Linezolid effectively stops the bacteria from multiplying, leading to their death. This mechanism makes it particularly effective against drug-resistant gram-positive bacteria.
Common Dosages
- 600 mg oral tablet or IV infusion every 12 hours for 10-14 days for most infections.
- The duration of treatment may vary depending on the type and severity of infection.
Typical Dosing
- For pneumonia: The typical dose is 600 mg every 12 hours for 10-14 days.
- For skin and soft tissue infections: The dose is also 600 mg every 12 hours for 10-14 days.
- For VRE infections: The treatment duration may be longer, typically 14-28 days depending on the infection site and severity.
- For pediatric patients, the dosing is based on body weight and can vary.
Typical Dosing
FDA Approved Indications
- Methicillin-resistant Staphylococcus aureus (MRSA) infections
- Vancomycin-resistant Enterococcus (VRE) infections
- Nosocomial pneumonia caused by Staphylococcus aureus (including MRSA)
- Community-acquired pneumonia caused by susceptible gram-positive bacteria
- Complicated and uncomplicated skin and soft tissue infections, including diabetic foot infections (without osteomyelitis)
Who Shouldn't Take Linezolid?
- Known hypersensitivity to linezolid or any of its components.
- Uncontrolled hypertension or pheochromocytoma, as linezolid has monoamine oxidase inhibitor (MAOI) properties, which can lead to hypertensive crises when used with certain medications or foods.
- Use of MAO inhibitors within the last 14 days, as this can increase the risk of serotonin syndrome and other serious interactions.
Advice From The Pharmacist
- Take Linezolid exactly as prescribed, with or without food. If using the oral suspension, shake the bottle well before each dose.
- Avoid consuming large amounts of tyramine-rich foods, such as aged cheeses, smoked meats, or fermented products, while taking Linezolid, as this can lead to hypertensive crises due to its MAOI properties.
- Inform your healthcare provider of all medications you are taking, as Linezolid can interact with a variety of drugs, particularly serotonergic agents like SSRIs and MAO inhibitors.
- Monitor for diarrhea, as this could indicate Clostridioides difficile-associated diarrhea (CDAD), a potentially serious side effect of antibiotic use.
- Finish the entire course of therapy, even if symptoms improve early, to ensure the infection is fully treated.
Side Effects of Linezolid
Common Side Effects
- Headache
- Nausea
- Diarrhea
- Vomiting
- Dizziness
- Thrombocytopenia (low platelet count), which can increase the risk of bleeding or bruising
Uncommon/Severe Side Effects
- Peripheral neuropathy or optic neuropathy (nerve damage in the hands, feet, or eyes), especially with prolonged use
- Serotonin syndrome, especially when used with other serotonergic drugs (e.g., SSRIs, SNRIs, MAO inhibitors)
- Lactic acidosis (a rare but serious condition involving a build-up of lactic acid in the body, causing muscle pain, breathing difficulties, and fatigue)
- Clostridioides difficile-associated diarrhea (CDAD), which can occur with nearly all antibiotics
Risks and Warnings of Linezolid
- Myelosuppression: Linezolid may cause a decrease in white blood cells, platelets, or red blood cells, especially when used for more than 2 weeks. Regular blood count monitoring is recommended, particularly in long-term use.
- Serotonin Syndrome: Linezolid has MAOI activity, meaning it can interact with SSRIs, SNRIs, tricyclic antidepressants, and MAO inhibitors to cause serotonin syndrome. Symptoms include confusion, agitation, rapid heart rate, and increased body temperature.
- Peripheral and Optic Neuropathy: Prolonged use (over 28 days) can lead to nerve damage, resulting in tingling, numbness, or vision problems. Patients should be monitored for any signs of neuropathy.
- Lactic Acidosis: Though rare, Linezolid may cause lactic acidosis. Symptoms include unexplained nausea, vomiting, fatigue, and difficulty breathing.
Interactions with Linezolid
Common Drug Interactions
- SSRIs, SNRIs, and MAO inhibitors: Using Linezolid with these medications can increase the risk of serotonin syndrome.
- Tyramine-rich foods: Consuming foods high in tyramine (such as aged cheese, smoked meats, or fermented foods) while taking Linezolid can cause dangerously high blood pressure.
- Adrenergic agents: Medications like pseudoephedrine or dopamine can increase blood pressure when used with Linezolid.
- Anticoagulants: Linezolid can increase the risk of bleeding when used with blood thinners like warfarin.
Alternatives to Linezolid
- Vancomycin: Commonly used for serious gram-positive infections, including MRSA, but is given intravenously.
- Daptomycin (Cubicin): An alternative for complicated skin infections and bacteremia caused by gram-positive organisms, including MRSA.
- Tigecycline (Tygacil): Used for resistant infections caused by both gram-positive and gram-negative bacteria, though it has a higher risk of gastrointestinal side effects.
- Tedizolid (Sivextro): A newer oxazolidinone antibiotic with a similar mechanism of action to Linezolid but fewer dosing requirements and potentially fewer side effects.
