INSTRUCTION SHEET
on Medical Application of Preparation
LEFLOBACT
Registration number:
Trade name for the preparation: Leflobact
International non-proprietary name: levofloxacin
Chemical name: (-)-(S)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7n-pirydo[
11,2,3-de]-1,4-benzoxazine-6-carboxylic acid .
Dosage form: film coated tablets.
Composition:
Active substance: levofloxacin (as levofloxacin hemihydrate) – 250mg or 500mg;
Auxiliary substances: calcium stearate, starch 1500, potato starch, crospovidone (kollidon CL-M), povidone (polyvinylpyrrolidone), lactose (milc sugar), talc, cellulose microcrystalline.
Shell: hypromellose (oxypropylmethylcellulose), hypromellose (oxypropylmethylcellulose), macrogol
(polyethylglycol 4000), titanium dioxide, thropeolin 0.
Description: round convexo-convexe 250 mg tablets in yellow film coating; 500 mg oval tablets with
yellow film coating
Pharmacotherapeutic group: antimicrobial group fluoro-quinolone.
ATC code: [J01MA12]
Pharmacological action
Pharmacodynamics: antibacterial preparation of fluoro-quinolone group. Levoflaxacin is a levorotatory isomer of ofloxacin. Levofloxacin blocks enzymes DNA-gyrase (topoisomerase II) and topoisomerase IV, breaks super-helimerization and linking of DNA disruptions, and causes deep morphological
changes in the cytoplasm, cell walls and membranes of bacteria.
Levofloxacin is active in relation to most strains of microorganisms both in vitro and in vivo:
Aerobic gram-positive microorganisms: Staphylococcus spp. (coagulase-negative, methicillinsensitive/moderately methicillin-sensitive strains), Staphylococcus aureus, Staphylococcus epidermidis
(methicillin-sensitive strains); Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus pneumoniae (penicillin-sensitive/moderately penicillin-sensitive/penicillin-resistant strains), Streptococcus
(groups С, G), Viridans group streptococci (penicillin-sensitive and penicillin-resistant strains); Enterococcus faecalis; Corynebacterium diphtheriae; Listeria monocytogenes;
Aerobic gram-negative microorganisms: Acinetobacter spp., Acinetobacter anitratus, Acinetobacter
baumannii, Acinetobacter calcoaceticus; Actinobacillus actinomycetemcoraitans; Citrobacter freundii,
Citrobacter diversus; Eikenella corrodens; Enterobacter spp., Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Enterobacter sakazakii; Escherichia coli; Gardnerella vaginalis; Haemophilus ducreyi, Haemophilus influenzae (ampicillin-sensitive/ampicillin-resistant strains), Haemophilus parainfluenzae; Helicobacter pylori; Klebsiella spp., Klebsiella oxytoca, Klebsiella pneumoniae; Moraxella catarrhalis; Morganella morganii; Neisseria gonorrhoeae (including penicillinaseproducing strains), Neisseria meningitidis; Pasteurella spp., Pasteurella canis, Pasteurella dagmatis,
Pasteurella multocida; Proteus mirabilis, Proteus vulgaris; Providencia spp., Providencia rettgeri, Providencia stuartii; Pseudomonas spp., Pseudomonas aeruginosa, Pseudomonas fluorescens; Salmonella
spp.; Serratia spp., Serratia marcescens;
Anaerobic microorganisms: Bacteroides fragilis; Bifidobacterium spp.; Clostridium perfringens;
Fusobacterium spp.; Peptostreptococcus spp.; Propionibacterium spp.; Veillonella spp.;
Other microorganisms: Bartonella spp.; Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis; Legioneila spp., Legionella pneumophila; Mycobacterium spp., Mycobacterium leprae,
Mycobacterium tuberculosis;
Mycoplasma hominis; Mycoplasma pneumoniae; Rickettsia spp.;
Ureaplasma urealyticum.
Pharmacokinetics: The preparation, administered per os, is promptly and fully absorbed (food intake
does not affect too much speed and completeness of absorption). Bioavailability is 99%. The time required to reach maximum concentration is 1-2 hours; when 250mg and 500mg are taken in, the maxi1
mum concentration is 2.8mcg/ml and 5.2mcg/ml correspondingly. Bonding with plasma proteins is 3040 %. The preparation easily penetrates organs and tissues: lungs, the mucous coat of bronchi, phlegm,
organs of genito-urinary system (including the prostate gland), bony tissue, cerebrospinal fluid, polymorphonuclear leukocytes, and alveolar macrophages. In the liver some insignificant part of the preparation is oxidized and/or desathetylized. It is egested unchanged basically by kidneys with urine by
means of glomerular filtration and tubular secretion. Renal clearance is 70% of the general clearance.
The half-period is 6-8hours. Less than 5% of levofloxacin is excreted as metabolites. After peroral intake of the preparation 70% of the administered dose is excreted by kidneys unchanged within 24
hours; 87% - within 48 hours; 4% can be found in the rectum within 72 hours.
Therapeutic indications: inflammatory infections caused by sensitive microorganisms
- of the lower respiratory tract (chronic bronchitis, pneumonia);
- of ENT-organs (sinusitis, otitis media);
- of genitourinary organs (including acute pyelonephritis, prostatitis, urogenital clamidiosis);
- of skin and soft tissues (maturated atheromas, abscesses, furuncles);
- as part of complex therapy for drug-resistant forms of tuberculosis.
Counter-indications: hypersensitivity, epilepsy, sinews disease under previous quinolones treatment,
pregnancy, lactation period, infancy and adolescence (younger than 18y.o.), renal dysfunctions: with
creatinine clearance less than 20ml/min or when under hemodialysis.
With special care:
Old age (there is high probability of the concomitant renal function depression), deficit of glucose-6phosphatedehydrogenase.
Dosage and method of administration: the preparation is administered per os, before meals or between meals, without chewing it, and washing it down with a lot of liquid (0.5 or one glass). When
chronic bronchitis is aggravated, 250-500mg of the preparation is used for 7-10 days once a day. For
community-acquired pneumonia 500mg of the preparation is used for 7-14 days once or twice a day.
For sinusitis 500mg of the preparation is used for 10-14 days once a day. For uncomplicated infections
of the urinary tract 250mg of the preparation is used for three days once a day.
For complicated infections of the urinary tract (including pyelonephritis) 250mg of the preparation is
recommended once a day for 7-10 days. For prostatitis 500mg of the preparation is prescribed once a
day for 28 days. For skin and soft tissues infections 250-500mg of the preparation s is used once or
twice a day for 7-14 day. For tuberculosis as part of complex therapy for drug-resistant forms of tuberculosis 500mg of the preparation is administered once or twice a day (500-1000mg/a day) for up to
three months.
Levofloxacin is basically excreted by kidneys, so for patients with renal dysfunctions the dosage of the
preparation should be low. The relevant information is contained in the following table:
Creatinine clearance
Per os dosage
500mg/24h
First dosage:
500mg
50 – 20ml/min
Next dosage:
250mg/24h
500mg/12h
First dosage:
500mg
Next:
250mg/12h
Leflobact in tablets as extension of a therapy course can be prescribed to the patients, who were initially introduced intravenously Leflobact infusion solution and who improved their condition, which enables to prescribe them Leflobact for per os administration.
Side effects:
From digestive system: nausea, vomiting, diarrhea (including diarrhea with blood discharge), digestion
disorders, loss of appetite, stomachaches, pseudomembranous enterocolitis; increase of activity of “hepatic” transminases, hyperbilirubinemia, hepatitis, dysbacteriosis.
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From cardiovascular system: low blood pressure, vascular collapse, lengthening of the interval Q-T.
Metabolism: hypoglycemia (appetite boost, excessive sweating, tremor).
From the central nervous system: headaches, dizziness, weakness, insomnia, tremor, anxiety, paresthesia, fears, hallucinations, confused mental state, depression, locomotory impairments, epileptic attacks
(among predisposed patients).
From sense organs: sight, hearing, or odor sense impairments; taste and tactile sensitivity disorders.
From locomotor system: arthralgia, muscle weakness, myalgia, tendon tear, tendinitis, rabdomyolis.
From urinary system: hypercreatininemia, interstitial nephritis, acute renal insufficiency.
From blood-forming organs: eosinophilia, hemolitic anemia, leucopenia, neutropenia, agranulocytosis,
thrombocytopenia, pancytopenia, hemorrhages.
Allergic reactions: itch and skin hyperemia, skin and mucous coat edemas, urticaria fever, StevensJohnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), bronchospasm, asphyxia, anaphylactic shock, allergic pneumonitis, vasculitis.
Other effects: asthenia, porphyria aggravation, photosensibilization, resistant fever, development of superinfection.
Overdose. Symptoms: nausea, erosive impairment of the mucous coat of the gastrointestinal tract,
lengthening of Q-T interval, mental confusion, dizziness, convulsions.
Treatment: gastric lavage, symptomatic treatment, dialysis is not effective. There is no specific antidote
for it.
Interaction with other pharmaceuticals:
The preparation increases the half-period of cyclosporine. The effect is reduced by the pharmaceuticals
that inhibit intestinal motility: sucralfate, aluminum- and magnesium-containing antacid pharmaceuticals and ferrum salts (an interval of not less than two hours is required between administrations).
Non-steroid anti-inflammatory preparations of ibuprofen group, theophyllin increase readiness for convulsions; glucocorticosteroids increase the risks of tendon tears.
Cimetidine and pharmaceuticals that block tubular secretion slow down excretion.
When levofloxacin is combined with the antagonists of vitamin K, control over coagulative hemic system is required.
Special warnings: after body temperature is normalized, therapy with the preparation should be continued for not less than 48-72 hours.
During treatment solar and artificial UV-radiation should be avoided to prevent from skin damage
(photosensibilization).
When signs of tendinitis or pseudomembranous colitis develop, levofloxacin should be immediately
cancelled.
It should be born in mind that patients with brain damage in their medical history (blood stroke, heavy
injury) can develop convulsions; by insufficiency of glucose-6-phosphatedehydrogenase there is the
risk of development of hemolysis.
While on therapy with the preparation, special care should be taken when driving or engaging in potentially hazardous types of activities that require mental concentration and high psychomotor ability.
Dosage form: 250mg or 500mg film coated tablets; 5, 7 or 10 250mg tablets or 5 or 7 500mg tablets
should be placed into a blister cellular pack.
7 or 10 250mg or 500mg tablets should be placed into polymeric cans. Each can or a blister cellular
pack with 7 or 10 250mg tablets; or 1 or 2 blister cellular pack with 5 250mg or 500mg tablets; or
1 blister cellular pack with 7 500mg tablets and application instructions should be placed into a cardboard box.
Storage:
List B. Store in a dry shadowed place at the temperature of not higher than 25°С. Keep out of reach of
children.
Shelf life: 3 years
Do not use after expiration date specified on the package.
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Dispensing form pharmacies: Prescription medicine.
Manufacturer/organization that accepts claims:
Open Joint Stock “Kurgan Joint Stock Company of Medical Preparations and Articles “Sintez” (Sintez
Joint Stock Company);
#7, Prospect Konstitutsii, city of Kurgan, Russian Federation, 640008;
Tel. /fax: (3522)481689
Internet-site: http://www.kurgansintez.ru
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