Linezolidin (linezolid) coated tablets 600 mg. №10

Description

Linezolidin composition
active ingredient: linezolid;
1 tablet contains linezolid based on 100% substance 600 mg;
auxiliary substances: microcrystalline cellulose; corn starch; hydroxypropyl cellulose; sodium starch glycolate (type A); magnesium stearate; coating mixture “Aquarius Preferred HSP BPP218011,” which contains hydroxypropylmethylcellulose, titanium dioxide (E 171), copovidone, polydextrose, polyethylene glycol, middle chain triglycerides.

Dosage form
Film coated tablets.

Pharmacological properties
Linezolidin is a synthetic substance, belongs to a new class of antimicrobial agents – oxazolidinones. It exhibits in vitro activity against aerobic gram-positive bacteria and anaerobic microorganisms. Linezolidin selectively inhibits the synthesis of bacterial proteins through a unique mechanism of action. It binds directly to the ribosomes of bacteria (23S from 50S subunits) and prevents the formation of a functional initiating complex 70S (an important component of the translation process).

Indications
Treatment of infections caused by sensitive strains of anaerobic and aerobic gram-positive microorganisms, including infections accompanied by bacteremia, such as:

• nosocomial pneumonia;
• nonhospital pneumonia;
• complicated infections of the skin and its structures, especially infections against the diabetic foot without concomitant osteomyelitis caused by Staphylococcus aureus (methicillin-sensitive and methicillin-resistant isolates), Staphylococcus pyogenes or Staphylococcus agalactiae;
• uncomplicated infections of the skin and its structures caused by Staphylococcus aureus (methicillin-sensitive isolates only) or Staphylococcus pyogenes;
• infections caused by enterococci, including vancomycin-resistant strains of Enterococcus faecium and faecalis.

If the agents of infection include gram-negative microorganisms, the purpose of combination therapy is clinically indicated.

Contraindications
Sensitivity to linezolid or any other component of the preparation is known.
Linezolidine should not be used in patients who take any drugs that suppress monoamine oxidase A and B (for example, phenelzine, isocarboxazide, selegiline, moclobemide), or within 2 weeks after taking such drugs.
Except where careful monitoring of blood pressure is possible, Linesolidine should not be prescribed to patients with the following concomitant clinical conditions or with concomitant administration of the following drugs:

• uncontrolled arterial hypertension, pheochromocytoma, carcinoid, thyrotoxicosis, bipolar depression, schizoaffective disorder, acute episodes of dizziness;
• serotonin reuptake inhibitors, tricyclic antidepressants, serotonin receptor 5-NT1 agonists (tryptans), direct and indirect sympathomimetics (including adrenergic bronchodilators, pseudoephedrine, phenylpropanolamine), vasopressors (epinephrine, norepinephrine), dopaminergic compounds (dopamine, dobutamine)

Children
The drug in this dosage form is prescribed for children from 12 years old.

Application during pregnancy or lactation
This drug is not recommended for use during these periods.

Method of administration and dosage
The duration of treatment depends on the pathogen, the location and severity of the infection, and the clinical effect of the therapy.
The recommendations for treatment duration, which are given below, have been applied in clinical trials. For some types of infections, a shorter duration of treatment may be appropriate, but this has not been evaluated in clinical studies.
The maximum duration of treatment is 28 days. The safety and efficacy of using Linezolidin for longer than 28 days has not been studied.
No increase in the recommended doses or duration of treatment is required in case of infections accompanied by bacteremia.

• Nosocomial, pneumonia, community-based pneumonia (in particular forms accompanied by bacteremia), complicated infections of the skin and its structures – 600 mg every 12 hours for 10-14 days;
• Infections caused by Enterococcus faecium resistant to vancomycin, in particular infections accompanied by bacteremia – 600 mg every 12 hours for 14–28 days;
• Uncomplicated infections of the skin and its structures
  Adults: 600 mg every 12 hours
  Children 12 years of age and older: 400 mg every 12 hours for 10-14 days.

The maximum dose for adults and children should not exceed 600 mg 2 times a day.

Overdose
The specific antidote is unknown.
There were no cases of overdose.
In case of an overdose, symptomatic treatment is indicated with measures to support the level of glomerular filtration. About 30% of the taken dose of the drug is eliminated within 3 hours of hemodialysis, but there is no data on the withdrawal of linezolid during peritoneal dialysis or hemoperfusion procedures. The two primary metabolites of linezolid are also cleared by hemodialysis.

Side effects:

• Infections and invasions: candidiasis, oral candidiasis, vaginal candidiasis, fungal infections; vaginitis.
• On the part of the blood and lymphatic system: anemia; leukopenia, neutropenia.
• From the side of metabolism and nutrition: hyponatremia.
• From the side of the psyche: insomnia.
• Neurological disorders: headache, taste perversion (metallic taste), dizziness.
• From the side of the organs of vision: blurred vision.
• From the organs of hearing and balance: ringing in the ears.
• From the heart: arrhythmia (tachycardia).
• From the side of the vessels: arterial hypertension.
• From the gastrointestinal tract: diarrhea, nausea, vomiting, local or generalized abdominal pain, constipation, dyspepsia; pancreatitis, gastritis, bloating, dry mouth, glossitis, frequent loose stools, stomatitis, upset or discoloration of the tongue.
• On the part of the hepatobiliary system: deviation from the norms of functional liver function tests, increased levels of ALT, AST or alkaline phosphatase.
• From the skin and subcutaneous tissue: itching, rash.
• From the kidneys and urinary system: an increase in blood urea nitrogen.
• General disorders and disorders at the injection site: fever, localized pain.

Shelf life
3 years.

Storage conditions
Store Linezolidin in its original packaging at a temperature not exceeding 25 ° C. Keep out of the reach of children.