Linezolid 2mg/ml Inj, 300ml
Overview
What is this medicine?
How to Use This Medicine
For proper storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to store this medication at home.
If you miss a dose, contact your doctor immediately to receive guidance on the appropriate course of action.
Lifestyle & Tips
- Avoid foods and beverages high in tyramine (e.g., aged cheeses, fermented meats, red wine, tap beer, soy sauce, sauerkraut) while taking linezolid and for two weeks after stopping it, as this can cause a dangerous increase in blood pressure.
- Limit consumption of caffeine-containing products.
- Avoid over-the-counter cold, flu, or diet medications that contain pseudoephedrine or phenylephrine without consulting your doctor or pharmacist.
- Inform your healthcare provider about all medications, supplements, and herbal products you are taking, especially St. John's Wort, as serious interactions can occur.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Condition-Specific Dosing:
Pediatric Dosing
Dose Adjustments
Renal Impairment:
Hepatic Impairment:
Pharmacology
Mechanism of Action
Pharmacokinetics
Absorption:
Distribution:
Elimination:
Pharmacodynamics
Safety & Warnings
Side Effects
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Allergic Reaction: Rash, hives, itching, red, swollen, blistered, or peeling skin with or without fever, wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Lactic Acidosis: Fast breathing, fast heartbeat, abnormal heartbeat, severe upset stomach or vomiting, excessive sleepiness, shortness of breath, feeling extremely tired or weak, severe dizziness, feeling cold, or muscle pain or cramps.
High Blood Pressure: Severe headache or dizziness, fainting, or changes in vision.
Low Blood Sugar: Dizziness, headache, feeling sleepy, weakness, shaking, rapid heartbeat, confusion, hunger, or sweating.
Low Sodium Levels: Headache, difficulty focusing, memory problems, confusion, weakness, seizures, or changes in balance.
Nerve Problems: Abnormal burning, numbness, or tingling sensations.
Vision Changes: Changes in eyesight.
Seizures: Convulsions or fits.
Low Blood Cell Counts: Increased risk of bleeding, infections, or anemia, especially in patients with bone marrow, kidney, or liver problems, or those taking certain other medications. If you experience signs of infection (fever, chills, sore throat), unexplained bruising or bleeding, or extreme fatigue or weakness, contact your doctor immediately.
C. diff-Associated Diarrhea (CDAD): Severe diarrhea that may be bloody, watery, or accompanied by stomach pain or cramps. CDAD can occur during or after antibiotic treatment and may lead to life-threatening bowel problems. If you experience any of these symptoms, contact your doctor right away.
Serotonin Syndrome: A potentially life-threatening condition that may occur when taking this medication with certain other drugs. Symptoms include agitation, changes in balance, confusion, hallucinations, fever, rapid or abnormal heartbeat, flushing, muscle twitching or stiffness, seizures, shivering or shaking, excessive sweating, severe diarrhea, upset stomach, or vomiting, or severe headache. Seek medical help immediately if you experience any of these symptoms.
Rhabdomyolysis: A severe muscle problem that may cause muscle pain or tenderness, muscle weakness, or dark urine. Contact your doctor right away if you experience any of these symptoms.
Other Side Effects
Most people do not experience severe side effects, but some may occur. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Headache
Diarrhea, upset stomach, or vomiting
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe or persistent diarrhea (may indicate C. difficile infection)
- Fever, chills, sore throat, or other signs of infection (may indicate myelosuppression)
- Unusual bleeding or bruising (may indicate low platelet count)
- Numbness, tingling, or burning pain in hands or feet (signs of peripheral neuropathy)
- Blurred vision, changes in color vision, or vision loss (signs of optic neuropathy)
- Nausea, vomiting, abdominal pain, or unexplained fatigue (signs of lactic acidosis)
- Confusion, agitation, hallucinations, rapid heart rate, sweating, tremor, or muscle stiffness (signs of serotonin syndrome)
- Severe headache, stiff neck, or sudden high blood pressure (signs of hypertensive crisis)
Before Using This Medicine
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ An adrenal gland tumor known as pheochromocytoma
+ High blood pressure
+ An overactive thyroid gland
If you have taken specific medications for depression or Parkinson's disease within the last 14 days, such as:
+ Isocarboxazid
+ Phenelzine
+ Tranylcypromine
+ Selegiline
+ Rasagiline
Note: Combining these medications with this drug can lead to severely high blood pressure.
This list is not exhaustive, and it is crucial to discuss all your medications and health conditions with your doctor. Please inform your doctor and pharmacist about:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
Your complete medical history
To ensure your safety, always verify with your doctor before starting, stopping, or changing the dose of any medication.
Precautions & Cautions
Monitor your blood pressure regularly, as directed by your doctor, since this medication can cause high blood pressure. Before using any over-the-counter (OTC) products, consult with your doctor, especially those that may raise blood pressure, such as:
Cough or cold medications
Diet pills
Stimulants
Non-steroidal anti-inflammatory drugs (NSAIDs), including ibuprofen or naproxen
* Certain natural products or aids
Some foods and beverages, like cheese and red wine, can cause a sudden and severe increase in blood pressure, which can be life-threatening. Discuss your risk with your doctor and obtain a list of foods and drinks to avoid during and after treatment, as advised by your doctor.
Regularly undergo blood work and other laboratory tests as directed by your doctor. Be aware that prolonged use of this medication (more than 28 days) can lead to severe eye problems, including loss of eyesight. Follow your doctor's recommendations for eye exams and discuss any concerns.
If you have diabetes (high blood sugar), inform your doctor, as this medication may lower blood sugar levels. Your diabetes medication may need to be adjusted. Monitor your blood sugar levels as directed by your doctor.
This medication can cause low sodium levels and a condition called syndrome of inappropriate antidiuretic hormone (SIADH) secretion, which can be severe and lead to breathing problems or even death. If you have questions or concerns, consult with your doctor.
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. Additionally, this medication may affect fertility in males, but this typically returns to normal after treatment is stopped. If you have questions, discuss them with your doctor.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
Overdose Information
Overdose Symptoms:
- Increased severity of known adverse effects (e.g., myelosuppression, neuropathy, gastrointestinal disturbances)
What to Do:
There is no specific antidote for linezolid overdose. Treatment should be supportive and symptomatic. Hemodialysis does not significantly remove linezolid. Contact a poison control center (e.g., 1-800-222-1222) or seek emergency medical attention immediately.
Drug Interactions
Contraindicated Interactions
- Monoamine Oxidase Inhibitors (MAOIs) (e.g., phenelzine, isocarboxazid, selegiline, tranylcypromine) - concurrent use or within 2 weeks of MAOI discontinuation due to risk of hypertensive crisis or serotonin syndrome.
- Certain serotonergic agents (e.g., SSRIs, SNRIs, TCAs, triptans, meperidine, tramadol, fentanyl, buspirone, St. John's Wort) - concurrent use is generally contraindicated due to risk of serotonin syndrome, unless the benefits outweigh the risks and the patient is closely monitored.
Major Interactions
- Adrenergic agents (e.g., pseudoephedrine, phenylephrine, dopamine, dobutamine, epinephrine, norepinephrine, vasopressors) - risk of hypertensive crisis due to MAO inhibition.
- Tyramine-rich foods/beverages (e.g., aged cheeses, fermented meats, red wine, tap beer, soy sauce, sauerkraut) - risk of hypertensive crisis.
- Myelosuppressive agents (e.g., methotrexate, azathioprine, chloramphenicol) - increased risk of myelosuppression (especially thrombocytopenia).
Moderate Interactions
- Anticoagulants (e.g., warfarin) - potential for increased bleeding risk (monitor INR).
- Antidiabetic agents (e.g., insulin, oral hypoglycemics) - theoretical risk of hypoglycemia due to MAO inhibition, though not well-established clinically.
- Other drugs causing lactic acidosis (e.g., metformin) - theoretical increased risk of lactic acidosis.
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Rationale: To establish baseline values and identify pre-existing myelosuppression, particularly thrombocytopenia, which is a known adverse effect.
Timing: Prior to initiation of therapy
Rationale: Although no dose adjustment is needed, to assess baseline kidney function.
Timing: Prior to initiation of therapy
Rationale: To assess baseline liver function.
Timing: Prior to initiation of therapy
Routine Monitoring
Frequency: Weekly, especially for patients receiving linezolid for more than 2 weeks or those with pre-existing myelosuppression or concurrent myelosuppressive drugs.
Target: Maintain platelet count > 75,000/mm³; hemoglobin and WBC within normal limits.
Action Threshold: Discontinue linezolid if significant myelosuppression occurs (e.g., platelet count < 75,000/mm³ or significant drop), or if clinically indicated.
Frequency: Periodically, especially if therapy extends beyond 28 days or if patient reports visual symptoms.
Target: Normal vision
Action Threshold: Discontinue linezolid if optic neuropathy or vision loss occurs.
Frequency: Periodically, especially if therapy extends beyond 28 days.
Target: Absence of numbness, tingling, or weakness.
Action Threshold: Discontinue linezolid if peripheral neuropathy develops.
Frequency: Monitor for signs/symptoms (e.g., recurrent nausea, vomiting, abdominal pain, unexplained acidosis).
Target: Normal acid-base balance
Action Threshold: Discontinue linezolid if lactic acidosis is confirmed or strongly suspected.
Frequency: Regularly, especially if co-administered with adrenergic agents or tyramine-rich foods.
Target: Normal blood pressure
Action Threshold: Manage hypertension if it occurs; consider discontinuing linezolid if severe.
Frequency: Closely monitor, especially if co-administered with serotonergic agents.
Target: Absence of mental status changes, autonomic instability, neuromuscular abnormalities, or GI symptoms.
Action Threshold: Discontinue linezolid and any serotonergic agents immediately if serotonin syndrome is suspected.
Symptom Monitoring
- Fever
- Sore throat
- Easy bruising or bleeding
- Unusual fatigue or weakness
- Numbness or tingling in hands or feet
- Blurred vision or changes in color perception
- Headache
- Dizziness
- Nausea
- Vomiting
- Diarrhea (especially severe or persistent)
- Abdominal pain
- Muscle pain or weakness
- Confusion
- Agitation
- Hallucinations
- Rapid heart rate
- Sweating
- Tremor
- Muscle rigidity
- Seizures
Special Patient Groups
Pregnancy
Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown developmental toxicity (reduced fetal body weights, skeletal ossification, and survival) at doses similar to or below human therapeutic exposures.
Trimester-Specific Risks:
Lactation
Linezolid and its metabolites are excreted into human milk. Due to the potential for serious adverse reactions in a breastfed infant (e.g., myelosuppression, mitochondrial toxicity), a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric Use
Dosing varies by age group (see detailedDosing). Safety and efficacy have been established in pediatric patients from birth through 17 years of age. Monitoring for adverse effects, particularly myelosuppression and neuropathy, is important.
Geriatric Use
No dose adjustment is necessary based on age. However, elderly patients may be more susceptible to adverse effects, particularly myelosuppression and neuropathy. Monitor closely.
Clinical Information
Clinical Pearls
- Linezolid is a valuable agent for treating serious Gram-positive infections, especially those caused by multidrug-resistant organisms like MRSA and VRE.
- Its excellent oral bioavailability (nearly 100%) allows for convenient IV-to-oral step-down therapy, which can facilitate earlier hospital discharge.
- The most significant adverse effects are myelosuppression (especially thrombocytopenia), peripheral neuropathy, and optic neuropathy, which are more common with prolonged therapy (typically >2 weeks). Regular CBC monitoring is crucial.
- Linezolid's MAOI activity necessitates careful consideration of drug-drug and drug-food interactions to avoid serotonin syndrome and hypertensive crises.
- It is bacteriostatic against staphylococci and enterococci, but bactericidal against most streptococci.
- Lactic acidosis is a rare but serious adverse effect, often associated with prolonged use and mitochondrial toxicity.
Alternative Therapies
- Daptomycin (for MRSA, VRE)
- Vancomycin (for MRSA, susceptible enterococci)
- Tigecycline (for MRSA, VRE, broad-spectrum)
- Ceftaroline (for MRSA)
- Quinupristin/Dalfopristin (for VRE faecium)
- Tedizolid (another oxazolidinone, similar spectrum, potentially lower myelosuppression risk)