Лефлобакт

General characteristics. Structure:

Active agent: levofloxacin (in the form of a levofloksatsin of a gemigidrat) – 250 mg or 500 mg; Excipients: calcium stearate, starch 1500, potato starch, кросповидон (коллидон CL-M), povidone (polyvinylpirrolidone), lactose (sugar milk), talc, cellulose microcrystallic. Cover: gipromelloz (oksipropilmetiltsellyuloz), macrogoal (polyethyleneglycol 4000), titanium dioxide, tropeolin 0.

Pharmacological properties:

Лефлобакт® - synthetic antimicrobic bactericidal drug of a broad spectrum of activity from group of ftorkhinolon.

Levofloxacin - left-handed isomer of an ofloksatsin. Levofloxacin blocks DNK-girazu enzymes (topoisomerase II) and topoisomerase IV, breaks superspiralling and a stitching of ruptures of DNA, causes profound morphological changes in cytoplasm, a cell wall and a membrane of bacteria.

Levofloxacin is active concerning the majority of strains of microorganisms as in the conditions of in vitro, and in vivo.

Gram-positive aerobic microorganisms: Staphylococcus spp. (koagulazonegativny, Methicillinum sensitive / moderately Methicillinum - sensitive strains), Staphylococcus aureus (Methicillinum - sensitive strains), Staphylococcus epidermidis (Methicillinum - sensitive strains), Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus pneumoniae (penicillin sensitive / it is moderate пенициллин-чувствительные/пенициллин-резистентные strains), Streptococcus spp (groups C, G), Streptococcus viridans (penicillin - sensitive and penicillin - resistant strains), Enterococcus faecalis, Corynebacterium diphtheriae, Listeria monocytogenes.

Gram-negative aerobic microorganisms: Acinetobacter spp. (including Acinetobacter anitratus, Acinetobacter baumannii, Acinetobacter calcoaceticus), Actinobacillus actinomycetemcomitans, Citrobacter freundii, Citrobacter diversus, Eikenella corrodens, Enterobacter spp. (including Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Enterobacter sakazakii), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (ампициллин-чувствительные/ампициллин-резистентные strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella catarrhalis, Morganella morganii, Neisseria gonorrhoeae (including penitsillinazoprodutsiruyushchy strains), Neisseria meningitidis, Pasteurella spp. (including Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (including Pseudomonas aeruginosa, Pseudomonas fluorescens), Salmonella spp., Serratia spp. (including Serratia marcescens).

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

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

 

Pharmacokinetics. Absorption

At intake drug is quickly and almost completely soaked up from a GIT. Meal influences the speed and completeness of absorption a little. Bioavailability - 99%. Tmax makes 1-2 h. At reception of 250 mg and 500 mg of Cmax makes 2.8 and 5.2 mkg/ml respectively.

Distribution

Linkng with proteins of plasma makes 30-40%. Well gets into bodies and fabrics: lungs, a mucous membrane of bronchial tubes, a phlegm, bodies of urinogenital system (including in a prostate), a bone tissue, cerebrospinal fluid, polymorphonuclear leukocytes, alveolar macrophages. Concentration of a levofloksatsin in lungs exceeds its concentration in a blood plasma.

Metabolism

In a liver a small part is oxidized and/or dezatsetilirutsya.

Removal

It is brought out of an organism in not changed view preferential with urine (by glomerular filtering and canalicular secretion). The renal clearance makes 70% of the general clearance. T1/2 makes 6-8 h. Less than 5% of a levofloksatsin are removed in the form of metabolites. After oral administration in not changed view with kidneys during 24 h 70% and for 48 h - 87% of the accepted dose are removed; in Calais during 72 h 4% are found.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to a levofloksatsin:

— lower respiratory tracts (chronic bronchitis, pneumonia);

— ENT organs (sinusitis, average otitis);

— urinogenital bodies (acute pyelonephritis, prostatitis, urogenital clamidiosis);

— skin and soft tissues (the suppurated atheromas, abscess, furuncles).

As a part of complex therapy of drug resistant forms of tuberculosis.

Route of administration and doses:

Drug should be accepted inside to food or in a break between meals, without chewing, washing down with enough liquid (from 0.5 to 1 glasses).

At an exacerbation of chronic bronchitis appoint 250-500 mg of 1 times / within 7-10 days.

At community-acquired pneumonia appoint on 500 mg 1-2 within 7-14 days.

At sinusitis appoint 500 mg of 1 times / within 10-14 days.

At uncomplicated infections of urinary tract appoint 250 mg of 1 times / within 3 days.

At the complicated infections of urinary tract (including pyelonephritis) - on 250 mg of 1 times / within 7-10 days.

At prostatitis appoint 500 mg of 1 times / within 28 days.

At infections of skin and soft tissues appoint on 250-500 mg 1-2 within 7-14 days.

As a part of complex therapy of drug resistant forms of tuberculosis appoint on 500 mg 1-2 (500-1000 mg/) up to 3 months.

Levofloxacin is removed preferential by kidneys therefore at treatment of patients with bounded function of kidneys it is required to reduce a drug dose.

Clearance of creatinine	Doses for intake
	500 mg / 24 h	500 mg / 12 h
	First dose: 500 mg	First dose: 500 mg
50 – 20 ml/min.	Then: 250 mg / 24 h	Then: 250 mg / 12 h

Leflobakt's appointment in the form of tablets for continuation of a course of treatment to those patients to whom at first it was appointed in/in Leflobakt's introduction in the form of solution for infusions is possible and the improvement of their state allowing to carry out further reception of a levofloksatsin inside was reached.

Features of use:

After normalization of body temperature it is recommended to continue treatment during not less than 48-72 h.

During treatment it is necessary to avoid solar and artificial UF-radiation in order to avoid damage of integuments (photosensitization).

At emergence of signs of a tendinitis, pseudomembranous colitis levofloxacin should be cancelled immediately.

At patients with damage of a brain in the anamnesis (including a stroke, a severe injury) development of spasms is possible; at insufficiency glyukozo-6-fosfatdegidrogenazy the risk of development of hemolysis increases.

Influence on ability to driving of motor transport and to control of mechanisms

During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From the alimentary system: nausea, vomiting, diarrhea (including with blood), digestion disturbance, a loss of appetite, an abdominal pain, a pseudomembranous coloenteritis, increase in activity of hepatic transaminases, a hyperbilirubinemia, hepatitis, dysbacteriosis.

From cardiovascular system: decrease in the ABP, vascular collapse, tachycardia, lengthening of an interval of QT.

From a metabolism: a hypoglycemia (including increase in appetite, the increased sweating, a shiver).

From a nervous system: a headache, dizziness, weakness, drowsiness, sleeplessness, a tremor, concern, paresthesias, fear, hallucinations, confusion of consciousness, a depression, motive frustration, epileptic seizures (at predisposed patients).

From sense bodys: vision disorders, hearing, sense of smell, flavoring and tactile sensitivity.

From a musculoskeletal system: arthralgia, muscular weakness, mialgiya, rupture of sinews, tendinitis, рабдомиолиз.

From an urinary system: giperkreatininemiya, intersticial nephrite, acute renal failure.

From system of a hemopoiesis: eosinophilia, hemolitic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhages.

Allergic reactions: itch and dermahemia, cutaneous dropsy and mucous membranes, small tortoiseshell, malignant exudative erythema (Stephens-Johnson's syndrome), toxic epidermal necrolysis (Lyell's disease), bronchospasm, suffocation, acute anaphylaxis, allergic pneumonitis, vasculitis.

Others: adynamy, porphyria aggravation, photosensitization, persistent fever, development of superinfection.

Interaction with other medicines:

At simultaneous use with Leflobakt cyclosporine T1/2 increases.

The medicines oppressing motility of intestines, сукральфат, aluminum-bearing and magniysoderzhashchy antiacid medicines and salts of iron at simultaneous use reduce Leflobakt's effect (the break between reception not less than 2 h is necessary).

At simultaneous use of Leflobakt with NPVS from group of an ibuprofen, theophylline convulsive readiness increases.

At simultaneous use of Leflobakt with GKS the risk of a rupture of sinews increases.

At simultaneous use of Leflobakt with Cimetidinum and medicines blocking canalicular secretion removal of a levofloksatsin from an organism is slowed down.

At a combination of a levofloksatsin with antagonists of vitamin K it is necessary to control a blood coagulation.

Contraindications:

— epilepsy;

— damage of sinews at earlier carried out treatment of a hinolonama;

— a renal failure at KK <20 ml/min.;

— hemodialysis;

— pregnancy;

— lactation period;

— children's and teenage age up to 18 years;

— hypersensitivity to drug components.

With care it is necessary to use drug at deficit glyukozo-6-fosfatdegidrogenazy, at patients of advanced age (high probability of existence of the accompanying depression of function of kidneys).

 

Use of the drug LEFLOBAKT® at pregnancy and feeding by a breast
Use of drug at pregnancy and during breastfeeding is contraindicated.

 

Use at renal failures
Use of drug at a renal failure at KK is contraindicated <20 ml/min., at stay on a hemodialysis.

 

Use for elderly patients
With care it is necessary to use drug at patients of advanced age (high probability of existence of the accompanying depression of function of kidneys).

 

Use for children
Drug is contraindicated to use at children's and teenage age up to 18 years.

Overdose:

Symptoms: nausea, erosive damages of mucous membranes of a GIT, lengthening of an interval of QT, confusion of consciousness, dizziness, spasms.

Treatment: symptomatic, a gastric lavage, dialysis it is inefficient. There is no specific antidote.

Storage conditions:

List B. Drug should be stored in the unavailable to children, dry, protected from light place at a temperature not above 25 °C. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

5 - planimetric strip packagings (1) - packs cardboard.
5 - planimetric strip packagings (2) - packs cardboard.
10 - planimetric strip packagings (1) - packs cardboard.