Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antimicrobial, refers 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 initiating complex 70S, which is a component of the translation process in protein synthesis.
It is active against aerobic Gram-positive bacteria: Corynebacterium jeikeium, Enterococcus faecalis (including glycopeptide-resistant strains), Enterococcus faecium (including glycopeptide-resistant strains), Enterococcus casseliflavus, Enterococcus gallinarum, Listeria monocytogenes, Staphylococcus aureus (including methicillin-resistant strains), Staphylococcus aureus (strains with intermediate sensitivity to glycopeptides), Staphylococcus epidermidis (including methicillin-resistant strains), Staphylococcus haemolyticus, Staphylococcus lugdunensis, Streptococcus agalactiae, Streptococcus intermedius, Streptococcus pneumoniae (including strains with intermediate sensitivity to penicillin and penicillin-resistant strains), Streptococcus spp. (Streptococcus groups C and G), Streptococcus pyogenes, Streptococcus viridans; aerobic gram-negative bacteria: Pasteurella canis, Pasteurella multocida; anaerobic Gram-positive bacteria: Clostridium perfringens, Peptostreptococcus spp. (including Peptostreptococcus anaerobius); anaerobic gram-negative bacteria: Bacteroides fragilis, Prevotella spp .; Chlamydia pneumoniae.
Less active against Legionella spp., Moraxella catarrhalis, Mycoplasma spp.
Not active against Haemophilus influenzae, Neisseria spp., Enterobacteriaceae, Pseudomonas spp.
There was no cross-resistance between linezolid and aminoglycosides, beta-lactam antibiotics, folic acid antagonists, glycopeptides, lincosamides, quinolones, rifamycins, streptograms, tetracyclines, chloramphenicol. The mechanism of action of linezolid differs from the mechanisms of action of these antibacterial drugs.
Resistance to linezolid develops slowly by a multistage mutation of 23S ribosomal RNA and occurs at a frequency of less than 1 Г— 10 -9 -1 Г— 10 -11 .
PHARMACOKINETICS
Linezolid is rapidly distributed in tissues with good perfusion. V d at achievement C ss at healthy volunteers makes on the average 40-50 l. Binding to plasma proteins is 31% and does not depend on the concentration of linezolid in the blood.
It is established that cytochrome P450 isoenzymes do not participate in the metabolism of linezolid in vitro. Linezolid also does not inhibit the activity of clinically important cytochrome P450 isoenzymes (1A2, 2C9, 2C19, 2D6, 2E1, 3A4). Metabolic oxidation leads to the formation of 2 inactive metabolites - hydroxyethylglycine (which is the main metabolite in humans and is formed as a result of a non-enzymatic process) and aminoethoxyacetic acid (formed in smaller amounts). Other inactive metabolites are also described.
Linezolid is excreted mainly with urine in the form of hydroxyethyl glycine (40%), aminoethoxyacetic acid (10%) and unchanged drug (30-35%). It is excreted in the form of hydroxyethyl glycine (6%) and aminoethoxyacetic acid (3%). The unchanged drug is practically not excreted with feces.
INDICATIONS
Treatment of infectious and inflammatory diseases caused by sensitive to anaerobic and aerobic gram-positive microorganisms (including infections accompanied by bacteremia): community-acquired pneumonia; hospital pneumonia; infections of the skin and soft tissues; infections caused by Enterococcus spp. (including Enterococcus faecalis and Enterococcus faecium strains resistant to vancomycin).
Infections caused by gram-negative microorganisms, confirmed or suspected (as part of combination therapy).
DOSING MODE
The dosage regimen and duration of treatment depends on the pathogen, the location and severity of the infection, and also on clinical effectiveness.
Enter IV in the form of infusions in a dose of 600 mg with an interval of 12 hours. Duration of treatment is 14-28 days.
Patients who at the beginning of the therapy the drug was assigned IV, in the future can be transferred to any dosage form for oral administration. At the same time, dose selection is not required, because bioavailability with oral administration is almost 100%.
SIDE EFFECT
On the part of the digestive system: often (> 1%) - perversion of taste, nausea, vomiting, diarrhea, abdominal pain (including spastic), flatulence, changes in bilirubin, ALT, AST, APF.
From the hemopoietic system: often (> 1%) - reversible anemia, thrombocytopenia, leukopenia, pancytopenia.
Other: often (> 1%) - headache, candidiasis; rarely cases of peripheral neuropathy and optic nerve neuropathy when used for more than 28 days (the link between the use of linezolid and the development of neuropathy has not been proven).
Adverse reactions are dose independent and, as a rule, do not require discontinuation of treatment.
CONTRAINDICATIONS
Hypersensitivity to linezolid.
PREGNANCY AND LACTATION
Adequate and strictly controlled studies of the safety of linezolid in pregnancy have not been conducted. The use of linezolid during pregnancy is only possible if the intended benefit of therapy for the mother exceeds the potential risk to the fetus
It is not known whether linezolid is excreted in breast milk, so if it is necessary to use the drug during lactation, breastfeeding should be discontinued.
SPECIAL INSTRUCTIONS
With the development of diarrhea against the background of the use of linezolid should take into account the risk of pseudomembranous colitis of varying severity.
In the process of treatment, it is necessary to conduct a clinical blood test in patients with an increased risk of bleeding, myelosuppression in anamnesis, as well as simultaneous use of drugs that reduce hemoglobin, platelet count or their functional properties, and in patients receiving linezolid for more than 2 weeks.
DRUG INTERACTION
Linezolid is a weak reversible nonselective inhibitor of MAO, therefore, in some cases linezolid is capable of causing a moderate reversible enhancement of the pressor action of pseudoephedrine and phenylpropanolamine. Considering this, with simultaneous application it is recommended to reduce initial doses of adrenergic drugs (including dopamine and its agonists) and further dose selection by titration.
