Levofloxacin tablets 500mg, No. 10

Infectious and inflammatory diseases caused by microorganisms sensitive to levofloxacin, including:

• acute bacterial sinusitis; lower respiratory tract infections (including exacerbation of chronic bronchitis, community-acquired pneumonia); infections of the urinary tract and kidneys (including acute pyelonephritis);

• chronic bacterial prostatitis;

• infections of the skin and soft tissues (festering atheroma, abscess, furunculosis);

• intra-abdominal infections in combination with drugs acting on the anaerobic microflora;

• tuberculosis (complex therapy of drug-resistant forms).

The drug is taken orally once or twice a day. The tablets should not be chewed and washed down with a sufficient amount of liquid (from 0.5 to 1 cup), can be taken before meals or between meals. Doses are determined by the nature and severity of the infection, as well as the sensitivity of the suspected pathogen.

Patients with normal or moderately reduced renal function (creatinine clearance> 50 ml / min) are recommended the following dosage regimen:

Acute bacterial sinusitis: 500 mg once a day for 10-14 days.

Exacerbation of chronic bronchitis: 250 mg or 500 mg once a day - 7-10 days.

Community-acquired pneumonia: 500 mg 1-2 times a day - 7-14 days.

Uncomplicated urinary tract infections: 250 mg once a day for 3 days.

Chronic bacterial prostatitis: 500 mg - 1 time per day - 28 days.

Complicated urinary tract infections, including pyelonephritis: 250 mg once a day for 7-10 days.

Skin and soft tissue infections: 250-500 mg 1-2 times a day - 7-14 days.

Intra-abdominal infection: 500 mg once a day - 7-14 days (in combination with antibacterial drugs acting on the anaerobic flora).

For tuberculosis (as part of complex therapy) - 500 mg 1-2 times a day, the course of treatment is up to 3 months.

Film-coated tablets of yellow color, round, biconvex, light yellow at a break; tablet weight 660 mg.

1 tab.

levofloxacin (in the form of hemihydrate) 500 mg

Excipients: croscarmellose sodium (primellose) 14 mg, magnesium stearate 6.4 mg, medium molecular weight polyvinylpyrrolidone 28 mg, microcrystalline cellulose 43.2 mg, colloidal silicon dioxide (aerosil) 10 mg, talc 12.8 mg, pregelatinized starch.

• Hypersensitivity to levofloxacin and other fluoroquinolones,

• epilepsy,

• damage to the tendons with previous treatment with quinolones,

• pregnancy, breastfeeding period,

• children and adolescents (up to 18 years old).

  Carefully

• Elderly age (a high probability of a concomitant decrease in renal function), deficiency of glucose-6-phosphate dehydrogenase.

pharmachologic effect

Levofloxacin is a broad-spectrum antimicrobial bactericidal agent from the group of fluoroquinolones. Blocks DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and stitching of DNA breaks, inhibits DNA synthesis, causes deep morphological changes in the cytoplasm, cell wall and membranes of bacteria.

Sensitive to the drug in vitro (minimum inhibitory concentration less than 2 mg / l):

Aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (leukotoxin-containing, coagulase-negative methicillin-susceptible / moderately susceptible strains), including Staphylococcus aureus (methicillin-susceptible strains), Staphylococcus epidermidis (methicillin-susceptible strains), Streptococcus spp. groups C and G, Streptococcus agalactiae, Streptococcus pneumoniae (penicillin-sensitive / moderately sensitive / resistant strains), Streptococcus pyogenes, Streptococcus spp. viridans group (penicillin-susceptible / resistant strains).

Aerobic gram-negative microorganisms: Acinetobacter spp. (including Acinetobacter baumannii), Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter spp. (including Enterobacter cloacae, Enterobacter aerogenes, Enterobacter agglomerans), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (ampicillin-susceptible / resistant strains), Haemophilus parainfluoblebsi. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella catarrhalis (beta-lactamase-producing and non-beta-lactamase-producing strains), Morganella morganii, Neisseria gonorrhoeae (including penicillinase-producing and non-producing strains, Pasisseria spp. (including Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis,Proteus vulgaris, Providencia spp. (incl. Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (including Pseudomonas aeruginosa), Salmonella spp., Serratia spp. (including Serratia marcescens).

Anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterium spp., Veilonella spp.

Other microorganisms: Bartonella spp., Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella pneumophila, Mycobacterium spp. (including Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma hominis, Mycoplasma pneumoniae, Ricketsia spp., Ureaplasma urealyticum.

Moderately sensitive microorganisms (minimum inhibitory concentration more than 4 mg / l):

Aerobic gram-positive microorganisms: Corynebacterium urealyticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis (methicillin-resistant strains), Staphylococcus haemolyticus (methicillin-resistant strains).

Aerobic gram-negative microorganisms: Burkholderia cepacia, Campylobacter jejuni, Campylobacter coli.

Anaerobic microorganisms: Bacteroides thetaiotaomicron, Bacteroides vulgatus, Bacteroides ovatus, Prevotella spp., Porphyromonas spp.

Resistant microorganisms (minimum inhibitory concentration over 8 mg / l):

Aerobic gram-positive microorganisms: Corynebacterium jeikeium, Staphylococcus aureus (methicillin-resistant strains), other Staphylococcus spp. (coagulase-negative methicillin-resistant strains).

Aerobic gram-negative microorganisms: Alcaligenes xylosoxidans.

Other microorganisms: Mycobacterium avium.

Pharmacokinetics

When taken orally, levofloxacin is rapidly and almost completely absorbed (food intake has little effect on the rate and completeness of absorption). Bioavailability - 99%. Time to reach Cmax in blood plasma - 1-2 hours; when taking 250 and 500 mg Cmax in blood plasma is about 2.8 and 5.2 ?g / ml, respectively. The connection with plasma proteins is 30-40%. It penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, organs of the genitourinary system, polymorphonuclear leukocytes, alveolar macrophages.

In the liver, a small portion is oxidized and / or deacetylated. Renal clearance is 70% of the total clearance. T1 / 2 - 8 hours. It is excreted from the body mainly by the kidneys by glomerular filtration and tubular secretion. Less than 5% of levofloxacin is excreted as metabolites. In unchanged form, 70% is excreted by the kidneys within 24 hours and 87% in 48 hours; the intestine removes 4% of the oral dose of levofloxacin within 72 hours.

Side effect

From the digestive system: nausea, vomiting, diarrhea (including blood), indigestion, loss of appetite, abdominal pain, pseudomembranous colitis; increased activity of hepatic transaminases, hyperbilirubinemia, hepatitis, dysbiosis.

From the side of the cardiovascular system: lowering blood pressure, vascular collapse, tachycardia, prolongation of the QT interval, atrial fibrillation.

From the side of metabolism: hypoglycemia (increased appetite, increased sweating, trembling, nervousness), hyperglycemia.

From the nervous system: headache, dizziness, weakness, drowsiness, insomnia, tremors, anxiety, paresthesia, fear, hallucinations, confusion, depression, movement disorders, convulsions.

From the senses: impairment of vision, hearing, smell, taste and tactile sensitivity.

From the musculoskeletal system: arthralgia, muscle weakness, myalgia, tendon rupture, tendonitis, rhabdomyolysis.

From the urinary system: hypercreatininemia, interstitial nephritis, acute renal failure.

From the side of hematopoiesis: eosinophilia, hemolytic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhages.

Allergic reactions: itching and flushing of the skin, edema of the skin and mucous membranes, urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), bronchospasm, dyspnea, anaphylactic shock, allergic pneumonitis, vasculitis.

Others: photosensitivity, asthenia, exacerbation of porphyria, persistent fever, development of superinfection.

Application during pregnancy and lactation

Contraindicated during pregnancy and breastfeeding.

Application in children

Contraindicated in children and adolescents (up to 18 years).

Use in elderly patients

Precautions: old age (high likelihood of a concomitant decrease in renal function).

special instructions

Levofloxacin is taken at least 2 hours before or 2 hours after taking aluminum or magnesium-containing antacids, or sucralfate, or other drugs containing calcium, iron or zinc salts.

During treatment, it is necessary to avoid the sun and artificial UV radiation in order to avoid damage to the skin (photosensitization).

When signs of tendinitis, pseudomembranous colitis, or allergic reactions appear, levofloxacin is immediately canceled.

It should be borne in mind that in patients with a history of brain damage (stroke, severe trauma), seizures may develop, with a deficiency of glucose-6-phosphate dehydrogenase, the risk of hemolysis increases.

In patients with diabetes mellitus, the concentration of glucose in the blood should be carefully monitored during treatment with levofloxacin.

With the simultaneous use of levofloxacin and warfarin, monitoring of prothrombin time, international normalized ratio or other anticoagulation tests is indicated, as well as monitoring for signs of bleeding. During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Overdose

Symptoms: nausea, erosive lesions of the mucous membranes of the gastrointestinal tract, prolongation of the QT interval, confusion, dizziness, convulsions.

Treatment: gastric lavage, symptomatic therapy, dialysis is not effective.

Drug interactions

Increases T1 / 2 of cyclosporine.

The effect of the drug is reduced by drugs that inhibit intestinal motility, sucralfate, aluminum and magnesium-containing antacid drugs and iron salts (a break between doses of at least 2 hours is required).

Non-steroidal anti-inflammatory drugs, theophylline increase the risk of seizures, glucocorticosteroids increase the risk of tendon rupture.

Cimetidine and drugs that block tubular secretion slow down excretion.

Hypoglycemic drugs: strict control over the concentration of glucose in the blood is necessary, since there is a possibility of hyper- and hypoglycemia when used simultaneously with levofloxacin.

Levofloxacin enhances the anticoagulant efficacy of warfarin.