Lebel - instructions for use, dose, side effects, contraindications

Composition:1 tablet, film-coated, contains:
active ingredient: levofloxacin hemihydrate, equivalent to levofloxacin 500 mg or 750 mg;
auxiliary ingredients:
for a dosage of 500 mg: microcrystalline cellulose 99.09 mg, hypromellose 5.60 mg, crospovidone 40.0 mg, sodium stearyl fumarate 16.85 mg; shell: Opaprai white (hypromellose, titanium dioxide, macrogol-400) 20.0 mg;
for a dosage of 750 mg: microcrystalline cellulose 147.66 mg, hypromellose 8.40 mg, crospovidone 60.0 mg, sodium stearyl fumarate 25.25 mg; shell: Opadrai white (hypromellose, titanium dioxide, macrogol-400) 30.0 mg.

Description:

Oval tablets covered with a film coating of white or almost white color, with a risk on one side. At the break, the core is from white with a yellow tinge to yellow.

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone

ATX: & nbsp

J.01.M.A Fluoroquinolones

J.01.M.A.12 Levofloxacin

Pharmacodynamics:

Levofloxacin is a synthetic fluoroquinolone with a broad spectrum of action. Inhibits DNA-gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA gaps, inhibits DNA synthesis, causes profound morphological changes in the cytoplasm,cell wall and membranes of sensitive microorganisms.

Levofloxacin is effective against most strains of the following microorganisms:

Aerobic Gram-positive microorganisms:

Corynebacterium diphtheriae, Enterococcus spp. (at t.h. Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (leukotoxin-containing and coagulase-negative methicillin-sensitive / moderately sensitive strains, incl. methicillin-sensitive strains Staphylococcus aureus and Staphylococcus epidermidis), Streptococcus spp. (at t.h. strains Streptococcus groups FROM and G, Streptococcus agalactiae, Streptococcus pyogenes, penicillin-sensitive / moderately sensitive/ resistant strains Streptococcus pneumoniae, penicillin- sensitive/resistant strains Streptococcus groups viridans).

Aerobic gram-negative microorganisms:

Acinetobacter spp. (at t.h. Acinetobacter baumannii), Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter spp. (at t.h. Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus spp. (at t.h. Haemophilus ducreyi, Haemophilus parainfluenzae, ampicillin- sensitive/resistant strains Haemophilus influenzae), Helicobacter pylori, Klebsiella spp. (at t.h. Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella catarrhalis (producing and non-reducing beta-lactamase strains), Morganella morganii, Neisseria spp. (at t.h. Neisseria meningitidis, producing and non-reducing penicillinase strains Neisseria gonorrhoeae), Pasteurella spp. (at t.h. Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida), Proteus spp. (at t.h. Proteus mirabilis, Proteus vulgaris), Providencia spp. (at t.h. Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (at t.h. Pseudomonas aeruginosa), Serratia spp. (at t.h. Serratia marcescens), Salmonella spp.

Anaerobic microorganisms:

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

Other microorganisms:

Bartonella spp., Chlamydia spp. (at t.h. Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis), Legionella pneumophila, Mycobacterium spp. (at t.h. Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma spp. (at t.h. Mycoplasma hominis, Mycoplasma pneumoniae), Rickettsia spp., Ureaplasma urealyticum.

Stable microorganisms:

Aerobic Gram-positive microorganisms:

Corynebacterium jeikeium, Staphylococcus spp. (coagulase-negative methicillin-resistant strains, including methicillin-resistant strains Staphylococcus aureus).

Aerobic Gram-negative microorganisms: Alcaligenes xylosoxidans.

Other microorganisms: Mycobacterium avium.

Pharmacokinetics:

Absorption: After oral administration levofloxacin quickly and almost completely absorbed from the gastrointestinal tract. Eating small affects the speed and completeness of absorption. Bioavailability is 99%.

The maximum concentration in plasma is achieved in 1-2 hours and for a dose of levofloxacin 250 mg, 500 mg and 750 mg is 2.8 μg / ml, 5.2 μg / ml, 8.0 μg / ml, respectively.

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

Metabolism: Levofloxacin is subject to limited metabolism in the liver (oxidation and / or deacetylation).

Excretion: It is excreted from the body mainly by the kidneys through glomerular filtration and tubular secretion. The half-life of levofloxacin is 6-8 hours. Less than 5% of the accepted dose is excreted in the form of desmethyl- and N-oxide metabolites. In unchanged form, 70% of the dose taken internally is excreted by the kidneys within 24 hours and 87% in 48 hours. 4% of the ingested dose is excreted by the intestine within 72 hours.

Indications:

Infectious-inflammatory diseases of mild and moderate severity caused by microorganisms sensitive to the preparation: infections of the lower respiratory tract (pneumonia, exacerbation of chronic bronchitis); acute bacterial sinusitis; urinary tract infection and kidney infection (including acute pyelonephritis); infections of the skin and soft tissues (festering atheromas, abscess, boils); chronic bacterial prostatitis; Intra-abdominal infection (in combination with antibacterial drugs acting on anaerobic microflora); tuberculosis (as part of complex therapy of drug-resistant forms).

Contraindications:

Hypersensitivity to levofloxacin, other fluoroquinolones, or other components of the drug in the anamnesis; epilepsy; the defeat of tendons associated with taking quinolones in an anamnesis; children and adolescents under 18; pregnancy; lactation period.

Carefully:

Elderly age (high probability of concomitant decrease in kidney function); deficiency of glucose-6-phosphate dehydrogenase.

Dosing and Administration:

Inside, before meals or at a break between meals, without chewing, squeezed enough water.

Adults with normal renal function (creatinine clearance greater than 50 ml / min) should be administered in accordance with the charts presented in the table:

Infection	Dose, mg	Multiplicity of reception per day	Duration treatment, days
Hospital pneumonia	750	1	7-14
Community-acquired pneumonia	500	1-2	7-14
Community-acquired pneumonia	750	1	5*
Acute bacterial exacerbation of chronic bronchitis	500	1	7
Acute bacterial sinusitis	500	1	10-14
Acute bacterial sinusitis	750	1	5
Uncomplicated urinary tract infections	250	1	3
Complicated urinary tract infections, incl. acute pyelonephritis	250	1	10**
	750	1	5***
Uncomplicated infections of the skin and subcutaneous tissue	500	1	7-10
Complicated infections of the skin and subcutaneous tissue	750	1	7-14
Chronic bacterial prostatitis	500	1	28
Intra-abdominal infection (in combination with antibacterial drugs acting on anaerobic microflora)	500	1	7-14
Tuberculosis (as part of complex therapy of drug-resistant forms)	500	1-2	Until 3 months

* This regimen is indicated for the treatment of community-acquired pneumonia caused by Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Mycoplasma pneumoniae, Chlamydia pneumoniae.

** The mode is shown for treatment infections urinary tract ways, caused by Enterococcus faecalis, Enterococcus cloacae, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa and acute pyelonephritis, caused by Escherichia coli.

*** The mode is shown for treatment infections urinary tract ways, caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and acute pyelonephritis, caused by Escherichia coli, including cases from concomitant bacteremia.

Correction of the dose of levofloxacin in adult patients with impaired renal function (creatinine clearance less than 50 ml / min)

Dose with normal kidney function every 24 hours	Creatinine clearance from 20 to 49 ml / min	Creatinine clearance from 10 to 19 ml / min	Clearance Creatinine less than 10 ml / min, incl. with hemodialysis or chronic outpatient peritoneal dialysis
750 mg	750 mg every 48 hours	The initial dose of 750 mg, followed by 500 mg every 48 hours	The initial dose of 750 mg, followed by 500 mg every 48 hours
500 mg	The initial dose is 500 mg, then 250 mg every 24 hours	The initial dose of 500 mg, followed by 250 mg every 48 hours	The initial dose of 500 mg, followed by 250 mg every 48 hours
250 mg	Correction of dose is not required	250 mg every 48 hours for uncomplicated infections urinary tract dosage adjustment is not required	No information on dose adjustment

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

Side effects:

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

From the sense organs: impaired vision, hearing, smell, taste and tactile sensitivity.

From the side of the cardiovascular system: lowering of arterial pressure, vascular collapse, tachycardia, lengthening of the interval Q-T, atrial fibrillation.

From the digestive system: nausea, vomiting, diarrhea (including with blood), digestive disorders, decreased appetite,abdominal pain, pseudomembranous colitis; increased activity of "hepatic" transaminases, hyperbilirubinemia, hepatitis, dysbacteriosis.

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 organs of hematopoiesis :, eosinophilia, hemolytic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhages.

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

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

Overdose:

Symptoms: nausea, erosive lesions of the mucous membranes of the gastrointestinal tract, lengthening of the interval Q-T, confusion, dizziness, convulsions.

Treatment: gastric lavage, if necessary - symptomatic therapy. There is no specific antidote, dialysis is ineffective.

Interaction:

Levofloxacin increases the half-life of cyclosporine.

The effect of levofloxacin reduces drugs that depress intestinal motility, sucralfate, aluminum- or magnesium-containing antacid drugs and iron preparations.

Non-steroidal anti-inflammatory drugs and theophylline at simultaneous use with levofloxacin increases the risk of seizures in predisposed patients, and glucocorticosteroids increase the risk of rupture of tendons.

With simultaneous administration of levofloxacin with hypoglycemic drugs, changes in blood glucose concentration, including hyperglycaemia and hypoglycemia, are possible.

Levofloxacin increases the anticoagulant effect of warfarin.

Cimetidine and drugs that block tubular secretion slow the withdrawal of levofloxacin.

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 ingestion of aluminum-or magnesium-containing antacids, or sucralfate, or other preparations containing calcium, iron or zinc.

Due to possible photosensitization during the treatment period and within 5 days after the end of levofloxacin treatment, sunlight and artificial ultraviolet irradiation should be avoided. With the development of phototoxicity, drug treatment should be discontinued.

When there are signs of tendonitis and pseudomembranous colitis levofloxacin immediately cancel.

It should be borne in mind that in patients with a history of brain damage (stroke, severe trauma) may develop seizures.

With insufficiency of glucose-6-phosphate dehydrogenase, the risk of hemolytic reactions is possible.

Patients with diabetes mellitus during treatment with levofloxacin should carefully monitor the concentration of glucose in the blood.

With the simultaneous use of levofloxacin and warfarin, monitoring of prothrombin time, international normalized ratio or other anticoagulation tests, as well as monitoring of bleeding symptoms, is shown.

Effect on the ability to drive transp. cf. and fur:

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

Form release / dosage:

Film coated tablets 500 mg and 750 mg.

Packaging:

7 tablets in the blister of (PVC / PE / PVDC) / aluminum. 1 blister with instructions for use in a pack of cardboard.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:4 years.
Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000270

Date of registration:17.02.2011

The owner of the registration certificate:Nobel Ilach Sanayi Ve Tidjaret A.Sh.Nobel Ilach Sanayi Ve Tidjaret A.Sh. Turkey

Manufacturer: & nbsp

NOBEL ILAC SANAYII VE TICARET, A.S. Turkey

Representation: & nbspNobel Ilach Sanayi Ve Tidjaret A.Sh.Nobel Ilach Sanayi Ve Tidjaret A.Sh.Russia

Information update date: & nbsp06.10.2015

Illustrated instructions

Instructions

Lebel® (Lebel®)