Assign to adults for the treatment of infections caused by microorganisms sensitive to the drug: community-acquired pneumonia; complicated skin and soft tissue infections; (For the above-mentioned infections, Levofloxacin should only be used when the use of other antibacterial agents that are usually recommended for the initial treatment of these infections is impractical or impossible); pyelonephritis, complicated urinary tract infections; chronic bacterial prostatitis.
Levofloxacin tablets Composition
active substance: 1 tablet contains 256.23 mg of levofloxacin hemihydrate, which is equivalent to 250 mg of levofloxacin;
excipients: hypromellose, crospovidone, microcrystalline cellulose, sodium stearyl fumarate, polyethylene glycol 6000, talc, iron oxide red (E172), iron oxide yellow (E172), titanium dioxide (E 171).
Levofloxacin tablets Dosage form
Basic physical and chemical properties: tablets of a round shape, coated, from light pink to light brown in color with a pink tint, the upper and lower surfaces of which are convex.
Levofloxacin tablets Pharmacotherapeutic group
Antibacterial agents for systemic use. Fluoroquinolones. Levofloxacin.
ATX code J01M A12.
Levofloxacin tablets Pharmacodynamics
Levofloxacin is a synthetic antibacterial drug from the group of fluoroquinolones, it is the S (-) enantiomer of the racemic mixture of the drug ofloxacin.
Mechanism of action. Levofloxacin as an antibacterial drug from the group of fluoroquinolones acts on the complex of DNA gyrase and topoisomerase IV
Pharmacokinetics / pharmacodynamics ratio. The degree of bacterial activity of levofloxacin depends on the ratio of the maximum serum concentration (max) or the area under the pharmacokinetic curve (AUC) and the MIC (inhibitory) concentration (MIC (MIC)).
The mechanism of resistance. Resistance to levofloxacin develops in a stepwise process due to target site mutations in both type II topoisomers, DNA gyrase and topoisomerase IV. Other mechanisms of resistance, such as an impenetrable barrier (common in Pseudomonas aeruginosa) and an eflux mechanism, can also affect sensitivity to levofloxacin.
Due to its mechanism of action, there is usually no cross-resistance between levofloxacin and other classes of antibacterial agents.
About 30-40% of levofloxacin binds to serum protein. The average volume of distribution of levofloxacin is approximately 100 liters after a single application and a repeated dose of 500 mg, which indicates a good distribution in body tissues.
Penetration into tissues and body fluids.
Levofloxacin has the ability to penetrate into the mucous membranes of the bronchi, bronchoalveolar fluids, alveolar macrophages, lung tissue, skin (blister content), prostate tissue and urine. Levofloxacin poorly penetrates the CSF.
Levofloxacin is metabolized to a very insignificant extent; the metabolites are dismethyl-levofloxacin and levofloxacin N-oxide. These metabolites make up less than 5% of the amount of the drug that is excreted in the urine. Levofloxacin is stereochemically stable and is not subject to chiral structure inversion.
After administration and administration, levofloxacin is slowly excreted from the blood plasma (half-life is 6-8 hours). The total clearance of levofloxacin after a single dose of 500 mg was 175 ± 29.2 ml / min. There is no significant difference in the pharmacokinetics of levofloxacin after intravenous and oral administration, indicating the interchangeability of these routes (administration and intravenous).