Levofloxacin is an antibacterial drug of broad-spectrum bactericidal action, blocks of methenolone – gyrase and topoisomerase of, inhibits the synthesis . The following is a summary of data on the activity of levofloxacin on the basis of studies in vitro and clinical findings.
Sensitive bacteria (minimum inhibitory concentration (MIC) ≤2 mg / ml) Aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus faecalis, Enterococcus spp, Listeria monocytogenes, Staphylococcus coagulase-negative methi-S (I). (methicillin-susceptible coagulase / -umerenno sensitive), Staphylococcus aureus methi-S(metitsillin- sensitive), of Staphylococcus epidermidis methi, the S (methicillin-sensitive), Streptococci group C and G, Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, Viridans streptococci. Aerobic gram-negative microorganisms: of Acinetobacter baumannii, of Acinetobacter spp,.Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter spp., Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae, Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella oxytoca, Klebsiella pneumoniae, Klebsiella spp., Moraxella catarrhalis, Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitidis, Pasteurella spp, Proteus mirabilis, Proteus vulgaris, Providencia . spp, Pseudomonas methenolone aeruginosa (nosocomial infections caused by Pseudomonas aeruginosa, can require the combined treatment), Pseudomonas spp,. Salmonella spp,. Serratia marcescens, Serratia spp. Anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp,. Fusobacterium spp,. of Propionibacterium spp,.Veilonella spp,. of Gardnerella vaginalis. Other micro-organisms: Bartonella spp,. of Chlamydophila pneumoniae, of Chlamydia psittaci, of Chlamydia trachomatis, of Legionella pneumophila, of Legionellaspp,. of Mycobacterium spp,. of Mycobacterium leprae, Micobacterium tuberculosis, of Mycoplasma pneumoniae, of Rickettsia spp. , . of Ureaplasma urealyticum moderately sensitive micro-organisms Aerobic gram-positive microorganisms: of Corynebacterium urealiticum, of Corynebacterium xerosis, of Enterococcus faecium, of Staphylococcus epidermidis methi, the R (methicillin-resistant), Staphylococcus haemolyticus methi-R. Aerobic gram-negative microorganisms: Burkholderia . cepacia, Campilobacter jejuni / coli Anaerobic microorganisms: Bacteroides thetaiotaomicron, Bacteroides vulgatus, Bacteroides ovatus, Prevotella spp,. Porphyromonas spp,. Peptostreptococcus, Clostridium perfringens.
Stable levofloxacin microorganisms Aerobic gram-positive microorganisms: Corynebacterium jeikeium , Staphylococcus aureus methi-R, Staphylococcus coagulase-negative methi-R. Aerobic gram-negative microorganisms: of Alcaligenes xylosoxidans, Burkholderia cepacia. Anaerobic microorganisms: of Bacteroides thetaiotaomicron, of Bacteroides fragilis. Other micro-organisms: . of Mycobacterium avium, of Mycoplasma hominis resistance resistance to levofloxacin occurs as a result phase process gene mutations encoding both types of topoisomerase II: DNA gyrase and topoisomerase IV (modification steps of the target). Other resistance mechanisms such as the mechanism of the effect on a penetration barriers microbial cells (mechanism characteristic of Pseudomonas aeruginosa) and efflux mechanism (active excretion of the antimicrobial agent from the microbial cells) may also reduce the sensitivity of microorganisms to levofloxacin. Between levofloxacin and other fluoroquinolone observed cross-resistance . in connection with the mechanism of action, cross resistance between levofloxacin and other groups antibacterial agents usually does not happen. The clinical effectiveness (efficacy in clinical trials for the treatment of infections caused listed below microorganisms) Aerobic gram-positive bacteria: Enterococcus faecalis, Staphylococcus aureus, Streptococcus . pneumoniae, Streptococcus pyogenes Aerobic gram-negative microorganisms: Citrobacter freundii, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella (Branhamella) catarrhalis, Morganella morganii, Proteus mirabilis, Pseudomonas aeruginosa, Serratia marcescens. Others: Chlamydia pneumoniae, Legionella pneumophila, Mycoplasma pneumoniae.
When administered levofloxacin is rapidly and almost completely absorbed from the gastrointestinal tract, bioavailability is approximately 99-100%. Maximum plasma concentrations are reached within 1-2 hours. food intake has almost no effect on the absorption of levofloxacin. Distribution Relationship to plasma proteins is 30-40%. After a single dose of 500 mg of levofloxacin is levofloxacin distribution volume is about 100 liters, indicating good drug penetration in human organs and tissues. The equilibrium concentration is reached within 48 h after administration of levofloxacin in a dose of 500 mg of 1 or 2 times per day. When administered 500 mg of levofloxacin: maximum concentration in bronchial mucosa and bronchial secretions are achieved after approximately 1 hour after drug administration and up 8.3 g / g and 10.8 micrograms / ml, respectively;maximum concentration achieved in lung tissue after 4-6 hours after dosing and approximately 11.3 ug / g. The concentration of drug in the lungs is greater than the concentration in the blood plasma.Levofloxacin penetrates poorly into cerebrospinal fluid. Metabolism Levofloxacin metabolized in small quantities to form the desmethyl-levofloxacin and levofloxacin-N-oxide. The share of these metabolites account for less than 5% of the dose excreted through the kidneys. Elimination of the drug is mainly carried out by the kidneys (more than 85% of the dose).
Infections caused by methenolone enanthate susceptible to levofloxacin strains of microorganisms:
• upper respiratory tract infections (acute sinusitis);
• lower respiratory tract infections (acute exacerbations of chronic bronchitis, community-acquired pneumonia);
• urinary tract infection;
• chronic bacterial prostatitis;
• Skin and soft tissue infections;
• in the complex therapy of drug-resistant forms of tuberculosis.