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

Excipients: calcium stearate, starch 1500, potato starch, crospovidone (kollidone CL-M), povidone (polyvinylpyrrolidone), lactose (milk sugar), talc, microcrystalline cellulose.

Sheath: hypromellose (hydroxypropylmethylcellulose), macrogol (polyethylene glycol 4000), titanium dioxide, tropeolin 0.

Description:

Tablets with a dosage of 250 mg - round biconvex form, covered with a film membrane of yellow color.

Tablets with a dosage of 500 mg are oval, covered with a film membrane of yellow color.

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone

ATX: & nbsp

J.01.M.A Fluoroquinolones

J.01.M.A.12 Levofloxacin

Pharmacodynamics:

Antibacterial drug of the group of fluoroquinolones. Levofloxacin is the left-handed isomer of ofloxacin. Levofloxacin blocks the enzymes DNA-gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA breaks, causes profound morphological changes in the cytoplasm, cell wall and bacterial membrane.

Levofloxacin is active against most strains of microorganisms both in conditions in vitro and in vivo:

Aerobic Gram-positive microorganisms: Staphylococcus spp. (coagulase-negative, methicillin-sensitive / 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 C, 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 actinomycetemcomitans; 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 penicillinase-producing 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; Legionella spp., Legionella pneumophila; Mycobacterium spp., Mycobacterium leprae, Mycobacterium tuberculosis; Mycoplasma hominis; Mycoplasma pneumoniae; Rickettsia spp.; Ureaplasma urealyticum.

Pharmacokinetics:

When ingested quickly and almost completely absorbed (eating little influence on speed and completeness of absorption). Bioavailability is 99%. The time required to reach the maximum concentration is 1-2 hours; when taking 250 mg and 500 mg, the maximum concentration is 2.8 and 5.2 μg / 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 (including the prostate gland), bone tissue, spinal fluid, polymorphonuclear leukocytes, alveolar macrophages.

In the liver, a small portion is oxidized and / or deacetylated.

It is excreted mainly from the kidneys with urine by glomerular filtration and tubular secretion in unchanged form. Kidney clearance is 70% of the total clearance. The half-life is 6-8 hours. Less than 5% of levofloxacin is excreted as metabolites. After oral administration unchanged with the kidneys within 24 hours, 70% are discharged and in 87 hours 87% of the dose taken; in the rectum in 4 hours found 4%.

Indications:

Infectious-inflammatory diseases caused by sensitive microorganisms:

- lower respiratory tract (chronic bronchitis, pneumonia);

- ENT organs (sinusitis, otitis media);

- urogenital organs (including acute pyelonephritis, prostatitis, urogenital chlamydia);

- skin and soft tissues (festering atheromas, abscess, boils);

- as part of complex therapy of drug-resistant forms of tuberculosis.

Contraindications:

Hypersensitivity, epilepsy, tendon damage with previously treated quinolones, pregnancy, lactation, children and adolescence (up to 18 years), renal dysfunction: with creatinine clearance less than 20 ml / min, when on hemodialysis.

Carefully:

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

Dosing and Administration:

Inside, before meals or in the interval between meals, without chewing, squeezed with enough liquid (0.5 to 1 cup).

With exacerbation of chronic bronchitis - 250-500 mg 1 time / day, for 7-10 days.

With community-acquired pneumonia - 500 mg 1-2 times / day, for 7-14 days.

With sinusitis - 500 mg 1 time / day, for 10-14 days.

With uncomplicated urinary tract infections: 250 mg once a day, for 3 days.

With complicated infections of the urinary tract (including pyelonephritis) - 250 mg 1 time / day, for 7-10 days.

With prostatitis - 500 mg 1 time / day, for 28 days.

For infections of the skin and soft tissues - 250-500 mg 1-2 times / day, for 7-14 days. With tuberculosis - as part of the complex therapy of drug-resistant forms of tuberculosis 500 mg 1-2 times / day (500-1000 mg / day) up to 3 months.

Levofloxacin is excreted mainly through the kidneys, therefore, in the treatment of patients with limited renal function, it is required to reduce the dose of the drug. Relevant information on this is provided in the following table:

Creatinine clearance	Doses for ingestion
	500 mg / 24 h	500 mg / 12 h
	First dose:	First dose:
	500 mg	500 mg
50 -20 ml / min.	Then: 250 mg/ 24 h	Then: 250 mg / 12 h

It is possible to prescribe Leflobact in tablets to continue the course of treatment for those patients who were first given an intravenous infusion of Leflobact and an improvement in their condition that allowed further administration of levofloxacin inside.

Side effects:

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

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

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

From the nervous system: headache, dizziness, weakness, drowsiness, insomnia, tremor, anxiety, paresthesia, fear, hallucinations, confusion, depression, movement disorders, epileptic seizures (in predisposed patients).

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

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

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

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

Allergic reactions: Itching and redness of the skin, 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: fatigue, aggravation of porphyria, photosensitivity, persistent fever, development of superinfection.

Overdose:

Symptoms include nausea, erosive lesions of the mucous membranes of the gastrointestinal tract (GIT), prolongation of the interval Q-T, confusion, dizziness, convulsions.

Treatment: gastric lavage, symptomatic, dialysis is ineffective.

There is no specific antidote.

Interaction:

Increases the half-life of cyclosporine.

The effect is reduced by drugs that depress intestinal motility, sucralfate, Aluminum and magnesium antacid drugs and salts of iron (interval between reception requires at least 2 hours).

Non-steroidal anti-inflammatory drugs (NSAIDs) from the ibuprofen group, theophylline increase the seizure, glucocorticosteroids (GCS) increase the risk of tendon rupture.

Cimetidine and drugs that block tubular secretion slow down excretion.

When levofloxacin is combined with vitamin K antagonists, control over the blood coagulation system is necessary.

Special instructions:

After normalization of body temperature, it is recommended to continue treatment for at least 48-78 hours.

During treatment, sun and artificial UV irradiation should be avoided to avoid damage to the skin (photosensitivity).

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

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

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

During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:The tablets covered with a film membrane, 250 mg, 500 mg.

Packaging:

For 5, 7 or 10 tablets with a dosage of 250 mg, 5 or 7 tablets with a dosage of 500 mg per circuit cell pack.

For 7 or 10 tablets with a dosage of 250 mg or 500 mg in a can of polymer.

Each jar, 1 circuit cell pack of 7 or 10 tablets with a dosage of 250 mg; 1 or 2 contiguous cell packs of 5 tablets with a dosage of 250 mg or 500 mg; 1 circuit cell pack of 7 tablets with a dosage of 500 mg with the instruction for use is placed in a pack of cardboard.

Storage conditions:

List B. In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005895/08

Date of registration:23.07.2008

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp26.10.2015

Illustrated instructions

Instructions

Leflobact (Leflobact)