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Linezolid 600 mg side effects: Linezolid: MedlinePlus Drug Information

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Linezolid – StatPearls – NCBI Bookshelf

Continuing Education Activity

Linezolid is a synthetic oxazolidinone antimicrobial drug. It is indicated for gram-positive infections and approved for the treatment of bacterial pneumonia, skin and skin structure infections, and vancomycin-resistant enterococcal (VRE) infections, including infections complicated by bacteremia. Linezolid does not have approval for the treatment of gram-negative infections, catheter-related bloodstream infections, or catheter site infections. Linezolid’s primary place in therapy is an alternative to vancomycin in inpatient settings. This activity covers linezolid so that members of the interprofessional team can recognize its indications, coverage, contraindications, and adverse event profile to optimally manage patients with an infectious disease and exercise appropriate antimicrobial stewardship.

Objectives:

  • Describe the mechanism of antimicrobial action for linezolid.

  • Summarize the indications for initiating linezolid therapy.

  • Explain the contraindications to using linezolid.

  • Review interprofessional team strategies for improving care coordination and communication to advance linezolid and improve outcomes.

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Indications

Linezolid is a synthetic oxazolidinone antimicrobial drug. It is indicated for gram-positive infections and approved for the treatment of bacterial pneumonia, skin and skin structure infections, and VRE infections, including infections complicated by bacteremia. Linezolid does not have approval for the treatment of gram-negative infections, catheter-related bloodstream infections, or catheter site infections.

Linezolid’s primary place in therapy is an alternative to vancomycin in inpatient settings. Vancomycin remains a standard treatment of methicillin-resistant Staphylococcus aureus (MRSA) infection. However, vancomycin-resistant isolates of S. aureus have emerged, and there are increasing reports of vancomycin-resistant isolates worldwide. Alternative treatment agents merit consideration before using linezolid in outpatient settings, as inappropriate use has led to an increase in linezolid-resistant vancomycin-resistant enterococci.[1]

Linezolid has activity against a broad range of antimicrobial susceptible and resistant gram-positive bacteria, including activity against MRSA with intermediate resistance to glycopeptides like vancomycin.  

Linezolid is a recommended empirical therapy option for MRSA in hospitalized adult patients with complicated skin and soft tissue infection, for community-associated MRSA skin and soft tissue infection, and MRSA-associated purulent and nonpurulent cellulitis. Linezolid is also an alternative option for MRSA in hospitalized pediatric patients.

Non-FDA uses include anthrax, bone and joint infections, brain abscess, febrile neutropenia, infectious arthritis, meningitis, orthopedic device-related infection, osteomyelitis, sepsis, subdural empyema, and ventriculitis.

Linezolid has demonstrated activity against most strains of the following microorganisms: Enterococcus faecalis, Enterococcus faecium, Pasteurella multocida, Staphylococcus aureus (MRSA and MSSA, i.e., methicillin-sensitive), Staphylococcus epidermidis, Staphylococcus haemolyticus, Streptococcus agalactiae (group B streptococci), Streptococcus pneumonia, Streptococcus pyogenes (group A beta-hemolytic streptococci), and viridians group streptococci (S. mutans, S. salivarius, S. anginosus, S. mitis, S. sanguinis, and S. bovis).[2][3]

Mechanism of Action

Linezolid is the first available oxazolidinone to inhibit bacterial protein synthesis by interfering with translation. Linezolid binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit, which prevents the formation of a functional 70S initiation complex.[4] This activity essentially inhibits protein production and prevents bacteria from multiplying.  

Linezolid is bacteriocidal against the majority of streptococcal strains and bacteriostatic against staphylococci and enterococci; this makes linezolid a poor option for immunosuppressed patients.

Linezolid is also a reversible, nonselective monoamine oxidase (MAO) inhibitor.[5] Monoamine oxidase inhibition leads to an increased concentration of the neurotransmitters epinephrine, norepinephrine, dopamine, and serotonin in the central and sympathetic nervous system. Inhibition can also lead to desensitization of alpha- and beta-adrenergic and serotonin receptors. In the gastrointestinal tract and liver, inhibition of MAO can result in systemic absorption of large amounts of tyramine from the diet and potentially cause life-threatening hypertension.

Administration

Linezolid is available in tablets, suspension, and injection. The dosage of intravenous (IV) and tablet formulations are interchangeable (there is no need to make dose adjustments). Renal dosing is not required. Invert gently to mix before administration, and do not vigorously shake oral suspension. Administer without regard to meals (food delays the rate but not the extent of oral absorption).

Administer linezolid IV infusion over 30 to 120 minutes. Do not mix or infuse with other medications. When using the same IV line for sequential infusion, flush the line with D5W, normal saline, or lactated Ringer’s solution before and after infusing linezolid. The yellow color of the injection may intensify with time without affecting potency.

Depending on the indication, the recommended dose is between 400 and 600 mg IV or orally every 12 hours for 10 to 28 days.

Absorption is rapid and extensive. Linezolid has excellent tissue penetration into the lungs and central nervous system and exhibits 100% oral bioavailability.[6]

Linezolid use may result in a suboptimal clinical response when treating organisms with a MIC (minimum inhibitory concentration) of 4 mcg/ml or greater and warrants a complete ID re-assessment and change in drug therapy.

Adverse Effects

The most common adverse effects experienced with linezolid use include decreased platelets, hemoglobin, and white blood cell counts, headache, nausea, diarrhea, elevated pancreatic enzymes, elevated liver function tests, and neuropathy.[7][8]

Warnings associated with linezolid include duration-related myelosuppression (thrombocytopenia, anemia, leukopenia), serotonin syndrome, hypoglycemia; caution in patients on insulin or hypoglycemic drugs, seizures, lactic acidosis, hypertension when used with adrenergic drugs, and irreversible peripheral and optic neuropathy when used for 28 days or greater; reports exist of blurred vision in patients receiving shorter courses of linezolid. Prolonged use may result in fungal or bacterial infection, including Clostridioides difficile-associated diarrhea (CDAD) and pseudomembranous colitis. CDAD can occur greater than two months postantibiotic treatment.

Lactic acidosis may also occur with use; therefore, evaluate patients who develop recurrent nausea and vomiting, unexplained acidosis, or low bicarbonate concentrations.

Contraindications

  • Do not use within two weeks of MAO inhibitors, e.g., phenelzine.

  • Avoid tyramine-containing foods and serotonergic drugs, as these may precipitate a hypertensive crisis. Examples of tyramine-containing foods include aged cheese, cured or smoked meats, draft beer, fava beans, and soy products.

  • Use caution with serotonergic and adrenergic drugs, e.g., imipramine.

Monitoring

Monitoring parameters include heart rate, blood pressure, blood glucose, weekly complete blood count (CBC), and visual function. Blood pressure requires close monitoring in patients with untreated hyperthyroidism. Patients with disease-related concerns such as diabetes mellitus, hypertension, hyperthyroidism, pheochromocytoma, and carcinoid syndrome also require close monitoring.

Toxicity

Toxicity is rare, and there is no antidote for linezolid. Symptomatic and supportive treatment is recommended for managing mild to severe toxicity.

For severe neutropenia, administer colony-stimulating factors such as filgrastim or sargramostim. Filgrastim 5 mcg/kg/day SQ or IV over 15 to 30 minutes, or sargramostim 250 mcg/m2/day IV over 4 hours. Transfusion of platelets, packed red cells, or both may be necessary for patients with severe thrombocytopenia, anemia, or hemorrhage.

For seizures, administer IV benzodiazepines; barbiturates or propofol may be an option if seizures persist or recur. Airway management may be necessary for patients with severe seizures. The primary treatment for serotonin syndrome is sedation with IV benzodiazepines and cooling measures (cyproheptadine is an option for milder cases). Activated charcoal is a consideration in patients with a recent overdose of linezolid tablets and co-ingested potentially dangerous medications, e.g., tricyclic antidepressants (must be alert and have a protected airway).

Monitoring is necessary for vital signs and liver enzymes in symptomatic patients. Additionally, monitor serial CBC with differential and platelet count. Reports exist of myelosuppression, including anemia, pancytopenia, leukopenia, and thrombocytopenia in patients receiving linezolid. Monitoring of serum electrolyte status is indicated for patients with significant diarrhea and/or vomiting. Also, monitor patients for clinical evidence of serotonin syndrome.

Enhancing Healthcare Team Outcomes

The healthcare team, e.g., physicians, nurses, and pharmacists, needs to work together to ensure that the patient correctly receives linezolid and is monitored for adverse drug reactions. Educate the patient about signs of significant adverse drug reactions, e.g., wheezing, chest tightness, seizures, swelling of the face, lips, tongue, or throat and severe diarrhea, etc. Encourage the patient to consult the healthcare team for questions about linezolid treatment. To prevent the inappropriate clinical use of linezolid, most hospitals have a committee that includes a pharmacist and an infectious disease expert who must first authorize its use.

Review Questions

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References

1.

Perry CM, Jarvis B. Linezolid: a review of its use in the management of serious gram-positive infections. Drugs. 2001;61(4):525-51. [PubMed: 11324682]

2.

Hamel JC, Stapert D, Moerman JK, Ford CW. Linezolid, critical characteristics. Infection. 2000 Jan;28(1):60-4. [PubMed: 10697798]

3.

Dresser LD, Rybak MJ. The pharmacologic and bacteriologic properties of oxazolidinones, a new class of synthetic antimicrobials. Pharmacotherapy. 1998 May-Jun;18(3):456-62. [PubMed: 9620097]

4.

Diekema DI, Jones RN. Oxazolidinones: a review. Drugs. 2000 Jan;59(1):7-16. [PubMed: 10718097]

5.

Antal EJ, Hendershot PE, Batts DH, Sheu WP, Hopkins NK, Donaldson KM. Linezolid, a novel oxazolidinone antibiotic: assessment of monoamine oxidase inhibition using pressor response to oral tyramine. J Clin Pharmacol. 2001 May;41(5):552-62. [PubMed: 11361052]

6.

Norrby R. Linezolid–a review of the first oxazolidinone. Expert Opin Pharmacother. 2001 Feb;2(2):293-302. [PubMed: 11336587]

7.

Clemett D, Markham A. Linezolid. Drugs. 2000 Apr;59(4):815-27; discussion 828. [PubMed: 10804037]

8.

Chien JW, Kucia ML, Salata RA. Use of linezolid, an oxazolidinone, in the treatment of multidrug-resistant gram-positive bacterial infections. Clin Infect Dis. 2000 Jan;30(1):146-51. [PubMed: 10619743]

Disclosure: Angela Azzouz declares no relevant financial relationships with ineligible companies.

Disclosure: Charles Preuss declares no relevant financial relationships with ineligible companies.

Apo-Linezolid – Uses, Side Effects, Interactions

How does this medication work? What will it do for me?

Linezolid belongs to the family of medications called antibiotics.  It is used to kill certain types of bacteria that cause infections in the abdomen, lungs (e.g., pneumonia), urinary tract, skin, and skin-structures (e.g., sweat glands, hair follicles). This medication works by killing bacteria or preventing their growth.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do.  It can be harmful for people to take this medication if their doctor has not prescribed it.

What form(s) does this medication come in?

Each white, oval, biconvex, film-coated tablet with “APO” engraved on one side and “LIN600” on the other, contains 600 mg of linezolid. Nonmedicinal ingredients: methyl cellulose, crospovidone, colloidal silicon dioxide, magnesium stearate, hydroxypropyl methylcellulose, hydroxypropyl cellulose, polyethylene glycol, and titanium dioxide.

How should I use this medication?

The recommended dose of linezolid depends on the type of infection being treated. For uncomplicated skin and skin-structure infections, the dose is usually 400 mg every 12 hours for 10 to 14 days. For most other types of infections, the usual dose is 600 mg every 12 hours for 10 to 14 days or for 14 to 28 days (depending on the type of infection being treated). The tablets may be taken with or without food.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is very important to take this medication exactly as prescribed by your doctor. Finish all this medication, even if you have started to feel better.

If you miss a dose of this medication, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication at room temperature, protect it from light and moisture, and keep it out of the reach of children.

Do not dispose of medications in wastewater (e. g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

Who should NOT take this medication?

Do not use this medication if you:

  • are allergic to linezolid or any ingredients of this medication
  • have taken monoamine oxidase (MAO) inhibitors (e.g., phenelzine, tranylcypromine) in the past 2 weeks
  • have uncontrolled high blood pressure
  • have untreated thyroid disease
  • have pheochromocytoma (tumour of the adrenal gland)
  • are taking medications that increase blood pressure (e.g., pseudoephedrine, epinephrine, dopamine)
  • are taking medications that affect the messenger serotonin (e.g., antidepressants, “triptan” migraine medications, buspirone)
  • have carcinoid syndrome (a group of symptoms which results from the release of hormones, such as serotonin, from carcinoid tumours)

What side effects are possible with this medication?

Many medications can cause side effects.  A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

  • change in colour of tongue
  • constipation
  • diarrhea
  • dizziness
  • dry mouth
  • headache
  • increased thirst
  • nausea
  • rash
  • stomach discomfort
  • taste changes
  • trouble sleeping
  • vomiting

Although most of the side effects listed below don’t happen very often, they could lead to serious problems if you do not seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

  • changes in vision (e.g., blurred vision, trouble seeing clearly)
  • fever or chills
  • increased blood pressure
  • ringing in the ears
  • symptoms of blood problems (unusual weakness or tiredness, unusual bleeding or bruising, shortness of breath, fever)
  • symptoms of high blood sugar (e.g., frequent urination, increased thirst, excessive eating, unexplained weight loss, poor wound healing, infections, fruity breath odour)
  • symptoms of low blood sugar (e.g., cold sweat, cool pale skin, headache, fast heartbeat, weakness)
  • symptoms of nerve problems (numbness, tingling, prickling, or burning sensations)
  • vaginal yeast infections (itching, white discharge)
  • white patches in the mouth or on the tongue or throat

Stop taking the medication and seek immediate medical attention if any of the following occur:

  • symptoms of antibiotic-associated diarrhea (severe, watery diarrhea that may be bloody)
  • symptoms of a severe allergic reaction (hives, difficulty breathing, swelling of the mouth or throat)
  • symptoms of a severe skin reaction such as blistering, peeling, a rash covering a large area of the body, a rash that spreads quickly, or a rash combined with fever or discomfort
  • symptoms of lactic acidosis (severe or recurrent nausea, vomiting, or diarrhea)
  • symptoms of serotonin syndrome (agitation, confusion, delirium, muscle stiffness, shaking, poor coordination, or seizures)

Some people may experience side effects other than those listed.  Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Are there any other precautions or warnings for this medication?

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Antibiotic-associated diarrhea: This medication, like other antibiotics, may cause a potentially dangerous condition called antibiotic-associated, or pseudomembranous, colitis. Symptoms include severe, watery diarrhea that may be bloody. If you notice these symptoms, stop taking linezolid and contact your doctor as soon as possible.

Bacterial resistance: Misuse of an antibiotic such as linezolid may lead to the growth of resistant bacteria that will not be killed by the antibiotic. If this happens, the antibiotic may not work for you in the future. Although you may begin to feel better early in your course of treatment with linezolid, you need to take the full course exactly as directed to finish ridding your body of the infection and to prevent resistant bacteria from taking hold. Do not take linezolid or other antibiotics to treat a viral infection such as the common cold; antibiotics do not kill viruses, and using them to treat viral infections can lead to the growth of resistant bacteria.

Diabetes: Linezolid may cause a loss of blood glucose control and glucose tolerance may change. People with diabetes may find it necessary to monitor their blood sugar more frequently while using this medication. Symptoms of low blood sugar include lightheadedness, weakness, cool, pale skin, or rapid heart rate.

If you have diabetes, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Foods with high tyramine content: When using this medication, avoid large quantities of foods or beverages with high tyramine content (e.g., draft beers, red wines, soy sauce, aged cheeses). The combination of linezolid and large amounts of tyramine may result in episodes of dangerously high blood pressure, which can be life-threatening.

Lactic acidosis: Rarely, linezolid may cause a serious condition called lactic acidosis (build-up of lactic acid in the blood). If you experience recurrent nausea or vomiting while taking this medication, get immediate medical attention.

Low blood cell counts: Linezolid may cause low blood cell counts. If you experience unusual weakness or tiredness, unusual bleeding or bruising, shortness of breath, or fever while taking linezolid contact your doctor immediately. Your doctor will monitor your blood cell counts while you are taking this medication.

Nerve problems: Linezolid may cause a nerve problem called peripheral neuropathy, especially when used for longer than recommended. If you experience numbness, tingling or prickling sensations, or burning pain while taking this medication, contact your doctor.

Other medical conditions: Linezolid may cause symptoms of other illnesses to become worse. If you have uncontrolled high blood pressure, pheochromocytoma, carcinoid syndrome, or untreated overactive thyroid, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Overgrowth of organisms: Treatment with antibiotics such as linezolid may allow normal fungus or types of bacteria not killed by the antibiotic to overgrow and cause unwanted infections such as yeast infections. Contact your doctor if you experience fever or chills while taking this medication.

Phenylketonuria: The oral liquid form of linezolid contains aspartame, an ingredient that cannot be broken down in the body by people who have phenylketonuria (a condition where you are lacking the enzyme needed to break down phenylalanine).  People with phenylketonuria should take linezolid tablets instead.

Seizures: This medication may cause seizures, especially for people with a history of seizures or who are at risk for seizures. Get immediate medical attention if you experience a seizure while taking this medication.

Serotonin syndrome: Severe reactions are possible when linezolid is combined with other medications that act on serotonin, such as tricyclic antidepressants and serotonin reuptake inhibitors, medications used to treat depression. These combinations must be avoided. Symptoms of a reaction may include muscle rigidity and spasms, difficulty moving, changes in mental state including delirium and agitation. Coma and death are possible.

If you are taking antidepressants, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Vision problems: Linezolid may cause vision problems, especially when used for longer than recommended. If you experience vision changes (e.g., blurred vision, changes in colour vision, trouble seeing clearly) while taking this medication, contact your doctor immediately.

Pregnancy: This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: This medication passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

Children: The safety and effectiveness of using this medication have not been established for children and adolescents less than 18 years old.

Seniors: People who are elderly may be more at risk of low sodium levels caused by linezolid.

What other drugs could interact with this medication?

There may be an interaction between linezolid and any of the following:

  • alcohol
  • amphetamines (e.g., dextroamphetamine, lisdexamfetamine)
  • antiemetics (e.g., granisetron, ondansetron)
  • antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
  • apraclonidine
  • atomoxetine
  • atropine eye drops
  • BCG
  • betahistine
  • bezafibrate
  • brimonidine
  • bromocriptine
  • fast acting bronchodilators (e.g., salbutamol, terbutaline)
  • long acting bronchodilators (e.g., formoterol, salmeterol)
  • buprenorphine
  • bupropion
  • buspirone
  • cabergoline
  • caffeine
  • carbamazepine
  • cholera vaccine
  • cladribine
  • cyclobenzaprine
  • decongestant cold medications (e.g., phenylephrine, pseudoephedrine)
  • decongestant eye drops and nose sprays (e. g., naphazoline, oxymetazoline, xylometazoline)
  • deferiprone
  • dexmethylphenidate
  • dextromethorphan
  • diabetes medications (e.g.,  acarbose, canagliflozin, glyburide, insulin, linagliptin, lixisenatide, metformin, rosiglitazone)
  • diphenoxylate
  • dipivefrin
  • disopyramide
  • domperidone
  • entacapone
  • epinephrine
  • ergot alkaloids (e.g., ergotamine, dihydroergotamine)
  • esketamine
  • hydroxychloroquine
  • lanreotide
  • levodopa
  • lithium
  • mesalamine
  • methadone
  • methyldopa
  • methylene blue
  • methylphenidate
  • metoclopramide
  • midodrine
  • mifepristone
  • mirtazapine
  • modafinil
  • monoamine oxidase (MAO) inhibitors (e.g., phenelzine, tranylcypromine, moclobemide, selegiline)
  • narcotic pain relievers (e.g., fentanyl, hydromorphone, morphine, oxycodone, tapentadol, tramadol)
  • octreotide
  • olsalazine
  • ozanimod
  • pasireotide
  • pizotifen
  • St. John’s wort
  • selective serotonin reuptake inhibitors (SSRIs, e.g., citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline)
  • serotonin agonists (“triptan” migraine medications; e.g., sumatriptan, zolmitriptan, rizatriptan, almotriptan)
  • serotonin/norepinephrine reuptake inhibitors (SNRIs; e.g., desvenlafaxine, duloxetine, venlafaxine)
  • sodium picosulfate
  • solriamfetol
  • sulfasalazine
  • sulfonamide antibiotics (“sulfas”; e.g., sulfadiazine, sulfamethoxazole)
  • tetrabenazine
  • theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
  • trazodone
  • tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, imipramine)
  • tryptophan
  • typhoid vaccine (oral)
  • warfarin

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

  • stop taking one of the medications,
  • change one of the medications to another,
  • change how you are taking one or both of the medications, or
  • leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications that you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.

All material copyright MediResource Inc. 1996 – 2023. Terms and conditions of use. The contents herein are for informational purposes only. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition. Source: www.medbroadcast.com/drug/getdrug/Apo-Linezolid

Averozolid 600 mg 10 tablets

Brand name:

Averozolid

Averozolid

Composition:

Each tablet contains:

Linezolid 600 mg

Auxiliary components:

corn starch – 66 mg, microcrystalline cellulose – 97 mg, povidone K30 – 14 mg, croscarmellose sodium – 17 mg, magnesium stearate – 8 mg, colloidal silicon dioxide – 4 mg, calcium hydrogen phosphate – 40 mg, sodium lauryl sulfate – 4 mg.

Features:

Antimicrobial agent, belongs to the class of oxazolidinones. The mechanism of action is due to selective inhibition of protein synthesis in bacteria. By binding to bacterial ribosomes, linezolid prevents the formation of a functional 70S initiation complex, which is a component of the translation process during protein synthesis.

Readings:

Treatment of infectious and inflammatory diseases caused by susceptible to anaerobic and aerobic gram-positive microorganisms (including infections accompanied by bacteremia): community-acquired pneumonia; hospital pneumonia; skin and soft tissue infections; infections caused by Enterococcus spp. (including strains of Enterococcus faecalis and Enterococcus faecium resistant to vancomycin). Infections caused by gram-negative microorganisms, confirmed or suspected (as part of combination therapy).

Dosage and administration:

The optimal dosage regimen is determined by the doctor. Compliance of the dosage form of a particular drug with indications for use and dosing regimen should be strictly observed.

On average, adults and children over 12 years of age take 600 mg every 12 hours, the duration of treatment is from 10 to 28 days

Children under 11 take 10mg/kg every 8 hours for 10 to 28 days.

Contraindications:

Hypersensitivity to linezolid.

Precautions:

With the development of diarrhea during the use of linezolid, the risk of developing pseudomembranous colitis of varying severity should be taken into account.

In the course of treatment, it is necessary to conduct a clinical blood test in patients with an increased risk of bleeding, a history of myelosuppression, as well as with simultaneous use of drugs that reduce hemoglobin levels, platelet count or their functional properties, as well as in patients receiving linezolid for more than 2 weeks.

Side effects:

From the digestive system: often – taste perversion, nausea, vomiting, diarrhea, abdominal pain (including spastic), flatulence, changes in total bilirubin, ALT, AST, alkaline phosphatase.

On the part of the hematopoietic system: often – reversible anemia, thrombocytopenia, leukopenia, pancytopenia.

Other: often – headache, candidiasis; rarely – cases of peripheral neuropathy and optic neuropathy when used for more than 28 days (the relationship between the use of linezolid and the development of neuropathy has not been proven).

Adverse reactions do not depend on the dose and, as a rule, do not require discontinuation of treatment.

Storage method:

In a dry cool place at a temperature not exceeding 30 degrees.

Packaging:

The cardboard box contains 1 blister of 10 tablets, paper instructions.

composition, indications, dosage, side effects

This drug belongs to the group of antibacterial drugs intended for systemic use.

The active ingredient in this drug is linezolid, a synthetic antibacterial agent that belongs to a new class of antimicrobial drugs, the oxazolidinins.

In vitro activity against Gram-positive aerobic, anaerobic and some Gram-negative bacteria and microorganisms.

Linezolid has the unique ability to selectively inhibit protein synthesis within bacterial cells.

Some types of enterococci, streptococci, staphylococci, as well as clostridia and other anaerobes with gram-positive activity are sensitive to linezolid. It is effective in the fight against some resistant microorganisms – hemophilic infection, others.

Composition and formulation

The main active ingredient of the drug is linezolid.

The following are used as auxiliary components: microcrystalline cellulose, corn starch, sodium starch glycolate, povidone, hydroxypropyl cellulose, magnesium stearate, hypromellose, dibatyl phthalate, talc, titanium dioxide, polyethylene glycol.

Produced in tablet form. One tablet contains 600 mg of linezolid.

Indications

This medicinal product is used in the treatment of infections caused by susceptible anaerobic and aerobic Gram-positive microorganisms, including those accompanied by bacteremia. In particular, such as:

– nosocomial pneumonia;

– community-acquired pneumonia;

– complicated infections of the skin and its structures, in particular infections against the background of diabetic foot without concomitant osteomyelitis, caused by Staphylococcus aureus (methicillin-sensitive and methicillin isolates), Streptococcus pyogenes or Streptococcus agalactiae;

– uncomplicated infections of the skin and its structures caused by Staphylococcus aureus (only methicillin-susceptible isolates) or Streptococcus pyogenes;

– Enterococcal infections, including vancomycin-resistant strains of Enterococcus faecium and faecalis.

If infectious agents include gram-negative organisms, combination therapy is recommended.

Contraindications

Not applicable if the patient has hypersensitivity (allergy) to one of the components that make up the drug.

Also contraindicated in:

– uncontrolled arterial hypertension;

– pheochromocytoma;

– carcinoid;

– thyrotoxicosis;

– bipolar depression;

– schizoaffective disorder;

– attacks of dizziness.

Concomitant use of any drugs that inhibit monoamine oxidase A and B (in particular phenelzine, isocarboxazid, selegiline, moclobemide), or within two weeks after taking such drugs.

Concomitant use with drugs – serotonin reuptake inhibitors, tricyclic antidepressants, serotonin 5-HT 1 receptor agonists (triptans), direct and indirect sympathomimetics (including adrenergic bronchodilators, pseudoephedrine, phenylpropanolamine), vasopressors (epinephrine, norepinephrine), dopaminergic compounds (dopamine, dobutamine), pethidine or buspirone.

Not for use in pediatric patients under 12 years of age.

Use in pregnancy and lactation

Not intended for use in pregnant women.

Also do not use during lactation.

Dosage and Administration

This drug is recommended to take 1 tablet of 600 mg 2 times a day, regardless of food intake.

The duration of treatment is determined by the attending physician, depending on the response of the patient’s body to treatment, the course of the disease.

The maximum duration of treatment is 28 days.

Recommended duration of treatment for:

– hospital and community-acquired pneumonia, complicated infections of the skin and its structures – 10-14 days;

– infections caused by Enterococcusfaecium resistant to vancomycin, in particular infections accompanied by bacteremia – from 14 to 28 days.

In the treatment of uncomplicated infections of the skin and its structures, the dosage for adults can be reduced to 400 mg 2 times a day, the duration of treatment is 10-14 days.

Elderly patients and patients with renal and hepatic insufficiency do not need to adjust the dosage and duration of treatment with this drug.

Overdose

No cases of overdose with this drug have been observed so far.

In case of overdose, hemodialysis is recommended to remove the drug from the body.

Side effects

Therapy with this drug may cause adverse reactions in the form of:

– oral, vaginal candidiasis, fungal infections, vaginitis, colitis, including pseudomembranous;

– eosinophilia, leukopenia, neutropenia, thrombocytopenia, myelosuppression, pancytopenia, sideroblastic anemia;

– anaphylactic shock;

– lactic acidosis, hyponatremia;

– insomnia;

– headache, taste perversion, dizziness, hypesthesia, paresthesia, serotonin syndrome, convulsions, peripheral neuropathy;

– visual impairment, optic neuritis, optic neuropathy, changes in color perception, visual sensations, visual field defect;

– ringing in the ears;

– arrhythmias, tachycardias;

– arterial hypertension, phlebitis, thrombophlebitis, transient ischemic attack;

– diarrhea, nausea, vomiting, abdominal pain, constipation, dry mouth, dyspepsia, gastritis, abdominal distension, glossitis, loose stools, pancreatitis, stomatitis, discoloration of the tongue;

– polyuria, renal failure;

– other adverse reactions.