Haileflox 500mg tablets, No. 5

Infectious and inflammatory diseases of mild and moderate severity caused by microorganisms sensitive to the drug:

• lower respiratory tract infections (pneumonia, exacerbation of chronic bronchitis);

• acute bacterial sinusitis; urinary tract and kidney infections (including acute pyelonephritis);

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

• chronic bacterial prostatitis;

• intra-abdominal infection (in combination with antibacterial drugs acting on the anaerobic microflora);

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

Reception mode is individual

Inside, before meals or between meals, without chewing, drinking plenty of water.

Film-coated tablets from light orange to orange, oval, biconvex, with a line on one side; at the fracture - a core from white with a yellow tint to yellow.

1 tab.

levofloxacin (in the form of hemihydrate) 500 mg

Excipients: corn starch, microcrystalline cellulose, povidone K30, methyl parahydroxybenzoate, propyl parahydroxybenzoate, purified talc, magnesium stearate, sodium carboxymethyl starch.

• Epilepsy;

• a history of tendon damage associated with the use of quinolones;

• children and adolescents up to 18 years old;

• pregnancy;

• lactation period;

• a history of hypersensitivity to levofoxacin, other fluoroquinolones or other components of the drug.

• The drug should be prescribed with caution in elderly patients (there is a high likelihood of a concomitant decrease in renal function), with a deficiency of glucose-6-phosphate dehydrogenase.

pharmachologic effect

Levofloxacin is a synthetic fluoroquinolone with a broad spectrum of action. Inhibits 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 sensitive microorganisms. Levofloxacin is active against aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (leukotoxin-containing and coagulase-negative methicillin-sensitive / moderately sensitive strains, including methicillin-sensitive strains Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus spp. ,penicillin-sensitive / moderately sensitive / resistant strains of Streptococcus pneumoniae, penicillin-sensitive / resistant strains of Streptococcus viridans); aerobic gram-negative microorganisms: Acinetobacter spp. (including Acinetobacter baumanii), Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter spp. (including Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus spp. (including Haemophilus ducreyi, Haemophilus parainfluenzae, ampicillin-sensitive / resistant strains of Haemophilus influenzae), Helicobacter pylori, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxela catarrhalis (strains producing and not producing ?-lactamase), Morganella morganii, Neisseria spp. (incl.Neisseria meningitidis, penicillinase-producing and non-penicillinase-producing strains of Neisseria gonorroeae), Pasteurella spp. (including Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida), Proteus spp. (including Proteus mirabilis, Proteus vulgaris), Providencia spp. (including Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (including Pseudomonas aeruginosa), Serratia spp. (including Serratia marcescens), Salmonella spp .; anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterum spp., Veilonella spp .; other microorganisms: Bartonella spp., Chlamydia spp. (including Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis), Legionella pneumophila, Mycobacterium spp. (including Mycobacterium leprae, Mycobacterium tuberculosis),Mycoplasma spp. (including Mycoplasma hominis, Mycoplasma pneumoniae), Rickettsia spp., Ureaplasma urealyticum. Aerobic gram-positive microorganisms are resistant to the drug: Corynebacterium jeikeium, Staphylococcus spp. (coagulase-negative methicillin-resistant strains, including methicillin-resistant strains of Staphylococcus aureus); aerobic gram-negative microorganisms: Alcaligenes xylosoxidans; other microorganisms: Mycobacterium avium.other microorganisms: Mycobacterium avium.other microorganisms: Mycobacterium avium.

Pharmacokinetics

Suction

After oral administration, levofloxacin is rapidly and almost completely absorbed from the gastrointestinal tract. Food intake has little effect on the rate and completeness of absorption. Bioavailability - 99%. Cmax in plasma is reached after 1-2 hours and for levofloxacin at doses of 250 mg, 500 and 750 mg is 2.8 ?g / ml, 5.2 ?g / ml and 8 ?g / ml, respectively.

Distribution

After taking a single or multiple dose, the amount of the absorbed drug is directly proportional to the dose taken. Css in plasma is reached after 48 hours. The average Vd of levofloxacin varies from 74 to 112 liters. Plasma protein binding 30-40%. It penetrates well into organs and tissues: lungs, bronchial mucosa, phlegm, alveolar macrophages (concentration in lung tissues is 2-5 times higher than plasma concentration), organs of the genitourinary system, polymorphonuclear leukocytes.

Metabolism

Levofloxacin undergoes limited metabolism in the liver (oxidation and / or deacetylation).

Withdrawal

It is excreted from the body mainly by the kidneys by glomerular filtration and tubular secretion. T1 / 2 of levofloxacin - 6-8 hours. Less than 5% of the dose taken is excreted in the form of desmethyl and N-oxide metabolites. In unchanged form, 70% of the dose taken orally is excreted by the kidneys within 24 hours and 87% - in 48 hours. 4% of the dose taken orally is excreted by the intestines within 72 hours.

Side effect

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 side of the cardiovascular system: decreased blood pressure, vascular collapse, tachycardia, prolongation of the QT interval, atrial fibrillation. 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 metabolism: hypoglycemia (increased appetite, increased sweating, trembling, nervousness). From the musculoskeletal system: arthralgia,muscle weakness, myalgia, rhabdomyolysis, tendon rupture, tendonitis. 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.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.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.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.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

The drug is contraindicated during pregnancy and lactation.

Application for violations of liver function

If liver function is impaired, dose adjustment is not required. the volume of metabolism of levofloxacin in the liver is limited.

Application in children

Contraindicated in children and adolescents under 18 years of age.

Use in elderly patients

The drug should be prescribed with caution in elderly patients (there is a high likelihood of a concomitant decrease in renal function).

special instructions

After normalization of body temperature, it is recommended to continue treatment for at least 48-72 hours. Levofloxacin is taken at least 2 hours before or 2 hours after taking magnesium / aluminum antacids, or sucralfate, or other drugs containing calcium, iron or zinc. Due to the possible photosensitization during the treatment period and within 5 days after the end of treatment with levofloxacin, solar and artificial ultraviolet irradiation should be avoided. If phototoxicity develops, drug treatment should be discontinued. When signs of tendinitis and pseudomembranous colitis appear, levofloxacin is immediately canceled. It should be borne in mind that patients with a history of brain damage (stroke, severe trauma) may develop seizures. With a deficiency of glucose-6-phosphate dehydrogenase, the risk of hemolytic reactions is possible.In patients with diabetes mellitus, blood glucose levels should be closely monitored during treatment with levofloxacin. With the simultaneous use of levofloxacin and warfarin, monitoring of prothrombin time, INR or other indicators of coagulation is indicated, as well as monitoring for signs of bleeding. Data on the use of Haileflox (750 mg) during radical or sparing sinusotomy in patients with chronic odontogenic perforated maxillary sinusitis indicates high clinical efficacy. Microbiological control of the use of the drug showed that the use of the drug at 750 mg 1 time / day for 10 days suppresses a number of aggressive bacteria that can cause infectious complications.The results obtained make it possible to recommend the drug Haileflox (750 mg) for the prevention of inflammatory complications of a sparing sinusotomy operation with plastic oroantral communication.

Influence on the ability to drive vehicles and use mechanisms

While taking levofloxacin, the patient's ability to concentrate and the speed of psychomotor reactions may be impaired. In this regard, care must be taken when driving vehicles and engaging in other potentially hazardous activities.

Overdose

Symptoms: nausea, erosive lesions of the mucous membranes of the gastrointestinal tract, prolongation of the QT interval, confusion, dizziness, convulsions. Treatment: gastric lavage, if necessary, symptomatic therapy. There is no specific antidote and dialysis is ineffective.

Drug interactions

Levofloxacin increases the T1 / 2 of cyclosporin. The effect of levofloxacin is reduced by drugs that inhibit intestinal motility, sucralfate, aluminum- or magnesium-containing antacid drugs and iron preparations. NSAIDs and theophylline, when used simultaneously with levofloxacin, increase the risk of seizures in predisposed patients, and GCS increase the risk of tendon rupture. With the simultaneous administration of levofloxacin with hypoglycemic drugs, changes in blood glucose levels, including hyperglycemia and hypoglycemia, are possible. Levofloxacin enhances the effect of warfarin. Cimetidine and drugs blocking tubular secretion slow down the excretion of levofloxacin.