Linezolid Canon, 200 mg 10 pcs

Antimicrobial agent, belongs to the class of oxazolidinones. Mechanism of action is due to selective inhibition of protein synthesis in bacteria. By binding to bacterial ribosomes linezolid prevents formation of functional initiating complex 70S, which is a component of translation process of protein synthesis.
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 penicillin-resistant strains 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.
No cross-resistance between linezolid and aminoglycosides, beta-lactam antibiotics, folic acid antagonists, glycopeptides, lincosamides, quinolones, rifamycins, streptogramines, tetracyclines, chloramphenicol is noted, since the mechanism of action of linezolid differs from that of other antibiotics. The mechanism of action of linezolid differs from that of these antibacterial agents.
Resistance to linezolid develops slowly by multistage mutation of 23S ribosomal RNA and occurs at a frequency of less than 1×10-9-1×10-11.
Pharmacokinetics
Linezolid rapidly distributes in tissues with good perfusion. Vd upon reaching Css in healthy volunteers averages 40-50 liters. Binding to plasma proteins is 31% and is independent of the blood concentration of linezolid.
Cytochrome P450 isoenzymes have not been shown to be involved in in vitro metabolism of linezolid. 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 by a non-enzymatic process) and aminoethoxyacetic acid (formed in smaller amounts). Other inactive metabolites are also described.
Linezolid is excreted mainly in the urine as hydroxyethylglycine (40%), aminoethoxyacetic acid (10%) and unchanged drug (30-35%). Excreted in the feces as hydroxyethylglycine (6%) and aminoethoxyacetic acid (3%). The unchanged drug is practically not excreted in the feces.

Indications

Active ingredient

Composition

Excipients: Betadex (betacyclodextrin) 10 mg, copovidone 9 mg, pregelatinized starch 18 mg, colloidal silica 3 mg, sodium stearyl fumarate 5 mg, magnesium hydroxycarbonate 28 mg.

Particle film coating: ready-made water-soluble film coating 7 mg (hypromellose 74.2%, talc 2.3%, polyethylene glycol 6000 14.3%, titanium dioxide 3.5%, iron oxide red dye 1.4%, iron oxide yellow dye 4.3%).

How to take, the dosage

Interaction

Special Instructions

Contraindications

Side effects

Overdose