Linezolid Canon pills 600mg, 10pcs

Composition

1 film-coated tablet,600 mg contains:

Active ingredient:

linezolid 600 mg;

Auxiliary substances:

corn starch 40 mg,

croscarmellose sodium 38 mg,

mannitol 54 mg,

magnesium stearate 8 mg,

povidone K-30 20 mg,

microcrystalline cellulose 100 mg;

Film shell:

opadraj white 26 mg, including:  hypromellose (hydroxypropylmethylcellulose) 8.775 mg, hyprolose (hydroxypropylcellulose) 8.775 mg, talc 5.2 mg, titanium dioxide 3.25 mg.

Indications

Treatment of infectious and inflammatory diseases if they are known or suspected to be caused by aerobic and anaerobic gram-positive microorganisms sensitive to linezolid (including infections accompanied by bacteremia):

• community-acquired pneumonia caused by Streptococcus pneumoniae (including multi-drug resistant strains), including cases accompanied by bacteremia, or Staphylococcus aureus (only methicillinsusceptible strains);
• hospital-acquired pneumonia caused by Staphylococcus aureus (including methicillinsusceptible and methicillin) or Streptococcus pneumoniae (including multi-drug resistant strains);
• complicated infections of skin and soft tissues, including infections in the diabetic foot syndrome is not accompanied by osteomyelitis, caused by Staphylococcus aureus (including methicillinsusceptible and methicillin), Streptococcus pyogenes and Streptococcus agalactiae;
• uncomplicated skin infections and soft tissue caused by Staphylococcus aureus (only methicillinsusceptible strains) or Streptococcus pyogenes;
• infections caused by Enterococcus faecalis (strains resistant to vancomycin), including, accompanied by bacteremia.

Contraindications

• • hypersensitivity to linezolid and/or other components of the drug;
  • children under 12 years of age (due to the inability to adequately select the dose);
  • simultaneous use with drugs that inhibit monoamine oxidase A or B (for example, phenelzine, isocarboxazide), as well as within two weeks after discontinuation of these drugs;

In the absence of careful monitoring of patients and monitoring of blood pressure, linezolid should not be prescribed:

• patients with uncontrolled hypertension, pheochromocytoma, hyperthyroidism, carcinoid syndrome, bipolar disorder, schizoaffective disorder and acute state of confusion;
• patients who receive the following types of drugs: sympathomimetic (eg, pseudoephedrine, phenylpropanolamine, epinephrine, norepinephrine, dobutamine), diaminopimelate (e. g., dopamine), inhibitors of serotonin reuptake, tricyclic antidepressants, agonists 5 HT 1 receptors (triptan), meperidine or buspirone.

Side effects

Infectious and parasitic diseasesOften-candidiasis (including oral candidiasis, vaginal candidiasis), fungal infections; infrequently-vaginitis; rarely-colitis caused by taking antibiotics (including pseudomembranous colitis).

Disorders of the blood and lymphatic systemOften-anemia; infrequently-leukopenia, neutropenia, thrombocytopenia, eosinophilia; rarely-pancytopenia; frequency unknown-myelosuppression, sideroblastic anemia.

Immune system disordersFrequency unknown – anaphylaxis.

Metabolic and nutritional disordersInfrequently-hyponatremia; frequency unknown-lactic acidosis.

Mental disordersOften include insomnia.

Nervous system disordersOften – headache, taste distortion (“metallic” taste in the mouth), dizziness; infrequently-convulsions, hyposthesia, parasthesia; frequency unknown-serotonin syndrome, peripheral neuropathy.

Visual disturbancesInfrequently – blurred vision; rarely-the appearance of visual field defects; frequency unknown – optic neuropathy, optic neuritis, vision loss, visual acuity change, color vision change.

Hearing disorders and labyrinth disordersInfrequently-ringing in the ears.

Disorders of the cardiovascular systemOften – increased blood pressure; infrequently: arrhythmia (tachycardia), transient ischemic attack, phlebitis, thrombophlebitis.

Gastrointestinal disordersOften – diarrhea, nausea, vomiting, localized or diffuse abdominal pain, constipation, dyspepsia; infrequently-pancreatitis, gastritis, bloating, dry mouth, glossitis, loose stools, stomatitis, discoloration of the tongue mucosa and other disorders of the tongue; rarely-superficial discoloration of tooth enamel.

Disorders of the liver and biliary tractOften – changes in the results of liver functional tests, increased activity of “liver enzymes” (including alanine aminotransferase (ALT), aspartate aminotransferase (ACT), alkaline phosphatase (ALP)), infrequently – an increase in the concentration of total bilirubin.

Skin disorders Often – rash, pruritus; infrequently-urticaria, dermatitis, excessive sweating; frequency unknown-bullous skin lesions (such as Stevens-Johnson syndrome, toxic epidermal necrolysis), angioedema, alopecia.

Disorders of the kidneys and urinary tractOften – increased blood urea concentration; infrequently-renal failure, increased plasma creatinine concentration, polyuria.

Genital and breast disordersInfrequently-disorders of the vagina and vulva.

General disorders and disorders at the injectionsite Often-fever, localized pain; infrequently-chills, weakness, thirst; pain at the injection site (for infusion solution).

How to take, course of use and dosage

The drug can be taken both during meals and between meals.

Patients who were prescribed intravenous linezolid at the beginning of therapy can then be transferred to linezolid dosage forms for oral use, while dose selection is not required, since the bioavailability of linezolid when taken orally is almost 100%.

The duration of treatment depends on the pathogen, the location and severity of the infection, as well as on the clinical effect.

Overdose

No overdose cases have been reported.

If necessary, symptomatic therapy is performed (including maintaining the glomerular filtration rate). Approximately 30% of the dose is eliminated within 3 hours on hemodialysis.

There are no data on accelerating the elimination of linezolid during peritoneal dialysis or hemoperfusion.

Special instructions

In an open-label study, among seriously ill patients with intravascular catheter-associated infections, there was an increase in mortality in patients treated with linezolid compared to patients treated with vancomycin/dicloxacillin/oxacillin [78/363 (21.5%) vs. 58/363 (16.0%)]. The main factor influencing mortality was the gram-positive pathogen of infection at the initial stage.

The mortality rate was similar among patients whose infections were caused only by gram-positive microorganisms, but was significantly higher in the linezolid group, when other microorganisms were detected, or they could not be detected at the initial stage. The greatest imbalance was observed during treatment and within 7 days after the end of antibiotic therapy. Many patients in the linezolid group were found to have gram-negative microorganisms during the study, and they died from infection caused by gram-negative microorganisms or polymicrobial infections.

Therefore, in the case of complicated skin and soft tissue infections, linezolid should be used in patients with known or possible co-infection with gram-negative microorganisms, only if there are no alternative treatment options. In these cases, additional use of drugs acting on gram-negative microflora is indicated simultaneously. Some patients taking linezolid may develop reversible myelosuppression (with anemia, thrombocytopenia, leukopenia, and pancytopenia), depending on the duration of therapy. Older patients also have an increased risk of developing this condition.

Thrombocytopenia was more common in patients with severe renal insufficiency, regardless of the use of hemodialysis in the patient. In this regard, during treatment, it is necessary to monitor blood parameters in patients with an increased risk of bleeding, a history of myelosuppression, as well as with the simultaneous use of drugs that reduce hemoglobin or platelet count and/or their functional properties, with severe renal insufficiency, as well as in patients taking linezolid for more than 2 weeks.

Linezolid in such patients is used only when careful monitoring of hemoglobin, white blood cell count and platelets is possible. If severe myelosuppression develops during linezolid therapy, treatment should be discontinued unless continuation of therapy is considered absolutely necessary. In this case, intensive monitoring of blood parameters and appropriate treatment is necessary.

In addition, it is recommended that a blood test (including the determination of hemoglobin, platelet count and white blood cells (with the calculation of the white blood cell formula)) It is performed weekly in patients receiving linezolid, regardless of the parameters of the initial blood test. A higher incidence of severe anemia was observed in patients treated with linezolid for more than the maximum recommended duration of 28 days. These patients were more likely to require blood transfusions. Cases of sideroblastic anemia were reported in the post-marketing period. In most cases, the duration of linezolid therapy exceeded 28 days. In most patients, the symptoms were fully or partially reversible after discontinuation of linezolid treatment with / without specific treatment for anemia.

Patients taking antibacterial drugs, including linezolid, should be considered for the risk of developing pseudomembranous colitis of varying severity. Cases of Clostridium difficile-related diarrhea have been reported in connection with the use of virtually all antibacterial drugs, including linezolid. The severity of diarrhea can range from mild to severe. Treatment with antibacterial drugs disrupts the normal intestinal microflora, which leads to excessive growth of Clostridium difficile. Clostridium difficile produces toxins A and B, which lead to the development of diarrhea associated with Clostridium difficile. Excessive amounts of toxins produced by Clostridium difficile strains can lead to increased mortality among patients, as such infections may be resistant to antimicrobial therapy, and colonectomy may also be required. Do not use medications that inhibit intestinal motility. The possibility of developing diarrhea associated with Clostridium difficile should be considered in all patients with diarrhea following the use of antibiotics. Close medical monitoring for 2 months is necessary for patients who have experienced diarrhea associated with Clostridium difficile after the introduction of antibacterial drugs.

If you experience symptoms of visual impairment, such as changes in visual acuity, changes in color perception, blurred vision, or visual field defects, it is recommended to consult an ophthalmologist immediately. Visual function should be monitored in all patients taking linezolid for a long time (more than 28 days), as well as in all patients with newly developed symptoms of visual impairment, regardless of the duration of therapy.

In the case of peripheral neuropathy and optic neuropathy, the risk/benefit ratio of continuing linezolid therapy in these patients should be evaluated. The risk of developing neuropathy is higher if linezolid is used in patients who are currently using or who have recently taken antibacterial drugs to treat tuberculosis. Lactic acidosis has been reported in association with the use of linezolid. Patients who experience repeated nausea or vomiting, abdominal pain, unexplained acidosis, or a decrease in the concentration of bicarbonate anions while taking linezolid should be carefully monitored by a doctor.

Linezolid inhibits mitochondrial protein synthesis. Side effects such as lactic acidosis, anemia, and neuropathy (peripheral and optic nerve) may occur as a result of this inhibition; these effects are more common when the drug is used for more than 28 days.

Seizures have been reported in patients taking linezolid, and in most cases there was a history of seizures or the presence of risk factors for their development. Patients should have a detailed medical history of previous episodes of seizures.

If it is necessary to use the drug in combination with selective serotonin reuptake inhibitors, patients should be constantly monitored for signs and symptoms of serotonin syndrome, such as impaired cognitive function, hyperpyrexia, hyperreflexia and impaired coordination of movements. If these symptoms occur, one or both medications should be discontinued. When stopping taking a serotonergic agent, symptoms of “withdrawal” syndrome may occur.

Cases of reversible surface discoloration of tooth enamel have been reported with linezolid. These discoloration changes were removed by professional tooth cleaning.

Cases of symptomatic hypoglycemia have been reported in diabetic patients treated with linezolid concomitantly with insulin or hypoglycemic drugs. Although a causal relationship between linezolid and hypoglycaemia has not been established, patients with diabetes should be warned about the possibility of hypoglycaemia. In case of hypoglycemia, it is necessary to adjust the dose of insulin/hypoglycemic drugs or cancel linezolid. Patients should be advised not to consume large amounts of food containing tyramine (such as red wine, old cheese, some alcoholic beverages, smoked meat).

No clinical studies have been conducted to study the effect of linezolid on the normal microflora of the human body.

The use of antibacterial drugs can sometimes lead to increased growth of non-susceptible microorganisms. Clinical studies have shown that approximately 3% of patients who received the recommended doses of linezolid developed candidiasis associated with taking antibiotics. If a superinfection occurs while taking linezolid, appropriate medical measures should be taken.

Clinical trials.

The safety and efficacy of linezolid with a duration of more than 28 days have not been established. Patients with diabetic foot syndrome, pressure sores or ischemic disorders, severe burns or gangrenous lesions were not included in controlled clinical trials. Thus, the experience of using linezolid in the treatment of these conditions is limited.

Influence on the ability to drive vehicles and mechanisms

During treatment, driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions are not recommended.

Active ingredient

Linezolid

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Indications

Skin Infections, Pneumonia