Linezolid 2mg/ml Sol For Inj 300ml

Manufacturer SUN PHARMACEUTICALS Active Ingredient Linezolid Injection(li NE zoh lid) Pronunciation li NE zoh lid
It is used to treat bacterial infections.
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Drug Class
Antibiotic
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Pharmacologic Class
Oxazolidinone
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Pregnancy Category
Category C
FDA Approved
Apr 2000
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Linezolid is an antibiotic used to treat serious bacterial infections, especially those caused by bacteria that are resistant to other common antibiotics, like MRSA (methicillin-resistant Staphylococcus aureus) and VRE (vancomycin-resistant Enterococcus). It works by stopping the growth of bacteria.
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How to Use This Medicine

To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Take this medication exactly as directed, and adhere to all guidelines provided. This drug is administered via infusion into a vein over a specified period of time.

If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the proper storage procedure.

In the event that you miss a dose, contact your doctor promptly to receive guidance on the appropriate course of action.
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Lifestyle & Tips

  • Avoid foods and beverages high in tyramine (e.g., aged cheeses, cured meats, fermented products, red wine, tap beer) while taking linezolid and for two weeks after stopping, as this can cause a dangerous increase in blood pressure.
  • Limit caffeine intake.
  • Report any new or worsening vision problems (blurred vision, changes in color vision, blind spots) immediately.
  • Report any new numbness, tingling, or weakness in your hands or feet immediately.
  • Report any unusual bleeding, bruising, fever, or signs of infection immediately.
  • Report any symptoms of serotonin syndrome (e.g., agitation, confusion, rapid heart rate, high blood pressure, fever, muscle stiffness, tremors, sweating, diarrhea) immediately, especially if taking other medications for depression or migraines.

Dosing & Administration

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Adult Dosing

Standard Dose: 600 mg IV every 12 hours
Dose Range: 600 - 600 mg

Condition-Specific Dosing:

Vancomycin-resistant Enterococcus faecium (VRE) infections: 600 mg IV every 12 hours for 14 to 28 days
Nosocomial pneumonia: 600 mg IV every 12 hours for 10 to 14 days
Complicated skin and skin structure infections (cSSSI): 600 mg IV every 12 hours for 10 to 14 days
Community-acquired pneumonia (CAP): 600 mg IV every 12 hours for 10 to 14 days
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Pediatric Dosing

Neonatal: Term neonates <7 days: 10 mg/kg IV every 12 hours. Term neonates ≥7 days: 10 mg/kg IV every 8 hours. Preterm neonates <7 days: 10 mg/kg IV every 12 hours. Preterm neonates ≥7 days: 10 mg/kg IV every 8 hours.
Infant: Birth to <12 years: 10 mg/kg IV every 8 hours (max 600 mg/dose).
Child: Birth to <12 years: 10 mg/kg IV every 8 hours (max 600 mg/dose).
Adolescent: ≥12 years: 600 mg IV every 12 hours.
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Dose Adjustments

Renal Impairment:

Mild: No dose adjustment required.
Moderate: No dose adjustment required.
Severe: No dose adjustment required.
Dialysis: No dose adjustment required. Linezolid and its metabolites are not significantly removed by hemodialysis or peritoneal dialysis. Administer dose after dialysis.

Hepatic Impairment:

Mild: No dose adjustment required.
Moderate: No dose adjustment required.
Severe: Use with caution in patients with severe hepatic impairment (Child-Pugh C) due to limited clinical data. No specific dose adjustment recommendations.

Pharmacology

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Mechanism of Action

Linezolid is an antibacterial agent of the oxazolidinone class. It inhibits bacterial protein synthesis by binding to the 23S ribosomal RNA of the 50S ribosomal subunit, thereby preventing the formation of a functional 70S initiation complex, which is essential for bacterial translation. This unique mechanism of action results in no cross-resistance with other antibiotic classes.
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Pharmacokinetics

Absorption:

Bioavailability: 100%
Tmax: Approximately 1 hour (oral)
FoodEffect: Food does not affect the absorption of linezolid.

Distribution:

Vd: 0.6-0.7 L/kg
ProteinBinding: Approximately 31%
CnssPenetration: Yes (achieves concentrations in CSF)

Elimination:

HalfLife: Approximately 4.5-5.5 hours
Clearance: Approximately 100 mL/min
ExcretionRoute: Renal (primarily as metabolites, some unchanged drug) and non-renal.
Unchanged: Approximately 30-35% (renal)
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Pharmacodynamics

OnsetOfAction: Rapid (within hours of administration)
PeakEffect: Within 1-2 hours post-infusion
DurationOfAction: Maintained for 12 hours with BID dosing due to time-dependent killing characteristics.
Confidence: High

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

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, irregular heartbeat, severe nausea or vomiting, excessive sleepiness, shortness of breath, extreme fatigue or weakness, 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, sleepiness, 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: Sudden, uncontrolled muscle contractions.
Low Blood Cell Counts: Increased risk of bleeding, infection, or anemia, especially in patients with bone marrow, kidney, or liver problems, or those taking certain medications. Seek medical help if you experience fever, chills, sore throat, unexplained bruising or bleeding, or extreme fatigue or weakness.
C. diff-Associated Diarrhea (CDAD): Severe, potentially life-threatening diarrhea that may occur during or after antibiotic treatment. Contact your doctor immediately if you experience stomach pain, cramps, or loose, watery, or bloody stools.
Serotonin Syndrome: A potentially life-threatening condition that may occur when taking this medication with certain other drugs. Seek medical help if you experience agitation, balance problems, confusion, hallucinations, fever, rapid or abnormal heartbeat, flushing, muscle twitching or stiffness, seizures, shivering or shaking, excessive sweating, severe diarrhea, nausea, or vomiting, or severe headache.
Rhabdomyolysis: A severe muscle problem that may cause muscle pain or tenderness, weakness, or dark urine. Seek medical help immediately if you experience these symptoms.

Other Side Effects

Most people experience few or no side effects while taking this medication. However, some common side effects may occur, including:

Headache
Diarrhea
* Nausea or vomiting

If these or any other side effects bother you or persist, contact your doctor or seek medical attention.

Reporting Side Effects

If you experience any side effects, you can report them to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. Your doctor can also provide guidance on managing side effects and answering any questions you may have.
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Seek Immediate Medical Attention If You Experience:

  • Severe headache, pounding in ears, blurred vision (hypertensive crisis)
  • Agitation, confusion, hallucinations, rapid heart rate, high blood pressure, fever, muscle rigidity, tremors, sweating, diarrhea (serotonin syndrome)
  • Unexplained nausea, vomiting, abdominal pain, hyperventilation (lactic acidosis)
  • Blurred vision, changes in color perception, visual field defects (optic neuropathy)
  • Numbness, tingling, burning, weakness in hands or feet (peripheral neuropathy)
  • Unusual bleeding or bruising, pale skin, extreme tiredness, shortness of breath, frequent infections (myelosuppression)
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

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 called 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 may lead to very 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 (OTC) 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 that it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Adhere to the prescribed duration of treatment, as using it for an extended period can increase the risk of a second infection.

Monitor your blood pressure regularly, as directed by your doctor, since this medication can cause high blood pressure. Before taking any over-the-counter (OTC) products, consult your doctor, especially those that may raise blood pressure, such as cough or cold medications, diet pills, stimulants, non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen or naproxen, and certain natural products or aids.

Some foods and drinks, including 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 for a specified period after treatment.

Regularly undergo blood work and other laboratory tests as instructed by your doctor. Be aware that prolonged use of this medication (beyond 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, inform your doctor, as this medication may lower blood sugar levels, potentially requiring adjustments to your diabetes treatment. Monitor your blood sugar levels as directed by your doctor.

This medication can also 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 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 temporarily affect fertility in males, but this typically returns to normal after stopping the medication. If you have questions, discuss them with your doctor.

It is crucial to inform your doctor if you are pregnant, plan to become pregnant, or are breastfeeding, as you will need to discuss the potential benefits and risks to you and your baby.
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Overdose Information

Overdose Symptoms:

  • Increased incidence and severity of known adverse effects (e.g., myelosuppression, neurological symptoms, lactic acidosis).

What to Do:

There is no specific antidote for linezolid overdose. Treatment should be supportive and aimed at maintaining glomerular filtration and renal function. 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

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Contraindicated Interactions

  • Patients taking any monoamine oxidase inhibitors (MAOIs) (e.g., phenelzine, isocarboxazid, selegiline, tranylcypromine) or within 2 weeks of taking an MAOI.
  • Patients with uncontrolled hypertension, pheochromocytoma, carcinoid syndrome, thyrotoxicosis, bipolar depression, schizoaffective disorder, acute confusional states, or taking other serotonergic drugs (e.g., SSRIs, SNRIs, TCAs, triptans, buspirone, meperidine, dextromethorphan, tramadol, St. John's Wort) unless close monitoring for serotonin syndrome is possible and benefits outweigh risks.
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Major Interactions

  • Serotonergic drugs (SSRIs, SNRIs, TCAs, triptans, buspirone, meperidine, dextromethorphan, tramadol, St. John's Wort): Risk of serotonin syndrome.
  • Adrenergic drugs (e.g., pseudoephedrine, phenylephrine, dopamine, epinephrine, norepinephrine): Potential for enhanced pressor response.
  • Tyramine-rich foods/beverages: Potential for hypertensive crisis (due to weak MAO inhibition).
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Moderate Interactions

  • Warfarin: Potential for increased INR/bleeding (monitor INR closely).
  • Rifampin: May decrease linezolid exposure (clinical significance uncertain, monitor for efficacy).
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Confidence Interactions

Monitoring

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Baseline Monitoring

Complete Blood Count (CBC) with platelet count

Rationale: To establish baseline and monitor for myelosuppression (thrombocytopenia, anemia, leukopenia).

Timing: Prior to initiation of therapy.

Visual acuity and color vision

Rationale: To establish baseline and monitor for optic neuropathy, especially with therapy >28 days.

Timing: Prior to initiation of therapy, if prolonged treatment is anticipated or patient has pre-existing visual impairment.

Neurological assessment

Rationale: To establish baseline and monitor for peripheral neuropathy, especially with therapy >28 days.

Timing: Prior to initiation of therapy, if prolonged treatment is anticipated.

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Routine Monitoring

Complete Blood Count (CBC) with platelet count

Frequency: Weekly, especially in patients receiving linezolid for >2 weeks, or those with pre-existing myelosuppression, or concomitant myelosuppressive drugs.

Target: Maintain within normal limits; Platelets >75,000/mm³.

Action Threshold: Discontinue linezolid if significant myelosuppression occurs (e.g., platelet count <75,000/mm³ or significant drop), or consider dose reduction/alternative therapy.

Signs and symptoms of serotonin syndrome

Frequency: Continuously, especially if co-administered with serotonergic agents.

Target: Absence of symptoms (agitation, hallucinations, tachycardia, labile blood pressure, hyperthermia, hyperreflexia, incoordination, nausea, vomiting, diarrhea).

Action Threshold: Discontinue linezolid and any serotonergic agents immediately if symptoms occur and initiate supportive care.

Signs and symptoms of lactic acidosis

Frequency: Continuously, especially if patient develops unexplained acidosis, nausea, vomiting, abdominal pain, or hyperventilation.

Target: Absence of symptoms.

Action Threshold: Discontinue linezolid if lactic acidosis is confirmed or strongly suspected.

Visual function (acuity, color vision, visual field)

Frequency: Periodically, especially if therapy extends beyond 28 days or if patient reports visual changes.

Target: Maintain baseline visual function.

Action Threshold: Discontinue linezolid if visual impairment occurs.

Neurological function (sensory/motor symptoms)

Frequency: Periodically, especially if therapy extends beyond 28 days or if patient reports new numbness, tingling, or weakness.

Target: Maintain baseline neurological function.

Action Threshold: Discontinue linezolid if peripheral neuropathy occurs.

Blood pressure

Frequency: Regularly, especially if co-administered with adrenergic agents or in patients with uncontrolled hypertension.

Target: Maintain within target range.

Action Threshold: Manage hypertension as needed; consider discontinuing linezolid if severe or uncontrolled.

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Symptom Monitoring

  • Unexplained nausea, vomiting, abdominal pain, hyperventilation (lactic acidosis)
  • Fever, sore throat, unusual bleeding/bruising, fatigue (myelosuppression)
  • Blurred vision, changes in color perception, visual field defects (optic neuropathy)
  • Numbness, tingling, burning, weakness in extremities (peripheral neuropathy)
  • Agitation, confusion, hallucinations, rapid heart rate, high blood pressure, fever, muscle rigidity, tremors, sweating, diarrhea (serotonin syndrome)

Special Patient Groups

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Pregnancy

Linezolid is classified as Pregnancy Category C. Animal studies have shown adverse effects on fetal development. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Trimester-Specific Risks:

First Trimester: Potential for developmental toxicity observed in animal studies (e.g., reduced fetal body weights, skeletal ossification delays).
Second Trimester: Potential for developmental toxicity observed in animal studies.
Third Trimester: Potential for developmental toxicity observed in animal studies.
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Lactation

Linezolid and its metabolites are excreted into human milk. Due to the potential for serious adverse reactions in breastfed infants (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.

Infant Risk: L3 (Moderate concern - Excreted into milk; potential for myelosuppression, mitochondrial toxicity, and gastrointestinal disturbances in infant. Monitor infant for feeding intolerance, diarrhea, rash, and signs of myelosuppression.)
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Pediatric Use

Linezolid is approved for use in pediatric patients from birth. Dosing is weight-based for younger children and adolescents. Safety and efficacy profiles are generally similar to adults, but specific monitoring for myelosuppression is important, especially in neonates and infants.

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Geriatric Use

No dose adjustment is required based on age. However, elderly patients may be more susceptible to adverse effects, particularly myelosuppression and neurological complications. Monitor closely for these effects.

Clinical Information

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Clinical Pearls

  • Linezolid is a bacteriostatic agent against staphylococci and enterococci, but bactericidal against most streptococci.
  • It is a weak, reversible, non-selective MAO inhibitor; therefore, strict dietary restrictions (tyramine-containing foods) and careful consideration of concomitant serotonergic/adrenergic medications are crucial.
  • Myelosuppression (especially thrombocytopenia) is a common and dose-limiting adverse effect, particularly with prolonged therapy (>2 weeks). Weekly CBC monitoring is essential.
  • Peripheral and optic neuropathy are rare but serious adverse effects, typically associated with prolonged therapy (>28 days). Patients should be advised to report any visual or neurological changes.
  • Lactic acidosis is a rare but potentially fatal adverse effect, thought to be related to mitochondrial toxicity. Discontinue if unexplained acidosis occurs.
  • Oral and IV formulations are 100% bioequivalent, allowing for easy IV-to-oral step-down therapy.
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Alternative Therapies

  • Daptomycin (for MRSA, VRE)
  • Vancomycin (for MRSA, susceptible Enterococcus)
  • Tigecycline (for cSSSI, CAP, VRE)
  • Ceftaroline (for MRSA cSSSI, CAP)
  • Quinupristin/Dalfopristin (for VRE faecium, cSSSI)
  • Tedizolid (another oxazolidinone, for cSSSI)
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Cost & Coverage

Average Cost: Varies widely by pharmacy and contract per 300ml bag (600mg)
Generic Available: Yes
Insurance Coverage: Tier 2 or 3 (preferred or non-preferred brand/generic)
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General Drug Facts

If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further guidance. To ensure safe use, never share your medication with others, and do not take medication prescribed to someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion.

Proper disposal of unused or expired medications is crucial. Do not dispose of them by flushing down the toilet or pouring down the drain unless specifically instructed to do so. If you are unsure about the correct disposal method, consult your pharmacist for advice. Many communities have drug take-back programs, which your pharmacist can help you locate.

Some medications may come with an additional patient information leaflet. Check with your pharmacist to see if this applies to your prescription. If you have any questions or concerns about your medication, do not hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider.

In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. Be prepared to provide detailed information about the overdose, including the name of the medication, the amount taken, and the time it occurred, to ensure prompt and effective treatment.