Leflobact pills 500mg, 10pcs

Composition

Core composition: Active ingredient: levofloxacin (in the form of levofloxacin hemihydrate) – 250 mg,500 mg; Excipients: calcium stearate – 3.7 mg,7.4 mg, starch 1500 – 18.5 mg,37.0 mg, potato starch – 31.8 mg,63.6 mg, crospovidone (collidone CL-M) – 7.4 mg,14.8 mg, povidone (polyvinylpyrrolidone low molecular weight medical 12600 ± 2700) – 5.8 mg,11.6 mg, lactose monohydrate (milk sugar) – 26.87 mg,53.73 mg, talc – 9.25 mg,18.5 mg, microcrystalline cellulose – 16.68 mg,33.36 mg;Shell composition: hypromellose (hydroxypropylmethylcellulose) – 17.7 mg,35.4 mg, macrogol (polyethylene glycol 4000) – 0.92 mg,1.84 mg, titanium dioxide-1.33 mg,2.66 mg, tropeolin 0-0.05 mg,0.1 mg

Pharmacological action

An antibacterial drug of the fluoroquinolone group. Levofloxacin is a levorotatory isomer of ofloxacin. Levofloxacin blocks the enzymes DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and crosslinking of DNA breaks, inhibits DNA synthesis, and causes deep morphological changes in the cytoplasm, cell wall, and membrane of bacteria. Levofloxacin is active against most strains of microorganisms, both in vitro and in vivo. vivo. In in vitroSensitive microorganisms (minimum inhibitory concentration (MPC) ≤ 2 mg / l; inhibition zone ≥ 17 mm)

Gram-positive aerobic microorganisms: Bacillus anthracis, Corynebacterium diphtheriae, Corynebacterium jeikeium, Enterococcus faecalis, Enterococcus spp., Listeria monocytogenes, Staphylococcus coagulase-negative methi-S(I) (coagulase-negative methicillin-sensitive/-moderately sensitive strains), Staphylococcus aureus methi-S (methicillin-sensitive strains), Staphylococcus epidermidis methi-S (methicillin-sensitive strains), Staphylococcus spp. CNS (coagulase-negative), Streptococci of groups C and G, Streptococcus agalactiae, Streptococcus pneumoniae peni I/S/R (penicillin-moderately sensitive/-sensitive/-resistant strains), Streptococcus pyogenes, Viridans streptococci peni S/R (penicillin-sensitive/-resistant strains).

Aerobic gram-negative microorganisms: Acinetobacter spp., Acinetobacter baumannii, Acinetobacter anitratus, Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter spp., Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae ampi-S/R (ampicillin-sensitive/ampicillin-resistant strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp., Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis β+/β- (reproducirse and producing beta-lactamase strains), Morganella morganii, Neisseria gonorrhoeae non-PPNG/PPNG (reproducirse and 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 (hospital infections caused by Pseudomonas aeruginosa may require combined treatment), 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.

Moderately sensitive microorganisms (MPC = 4 mg / l; inhibition zone 16-14 mm)

Gram-positive aerobic microorganisms: Corynebacterium urealyticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis methi-R (methicillin-resistant strains), Staphylococcus haemolyticus methi-R (methicillin-resistant strains).

Gram-negative aerobic microorganisms: Campylobacter jejuni / coli.

Anaerobic microorganisms: Prevotella spp., Porphyromonas spp.

Levofloxacin-resistant microorganisms (BMD ≥ 8 mg / l; inhibition zone ≤ 13 mm)

Gram-positive aerobic microorganisms: Staphylococcus aureus methi-R (methicillin-resistant strains), Staphylococcus coagulase-negative methi-R (coagulase-negative methicillin-resistant strains).

Gram-negative aerobic microorganisms: Alcaligenes xylosoxidans.

Anaerobic microorganisms: Bacteroides thetaiotaomicron.

Other microorganisms: Mycobacterium avium.

ResistanceResistance to levofloxacin develops as a result of a gradual process of mutations in the genes encoding both type II topoisomerases: DNA gyrase and topoisomerase IV. Other mechanisms of resistance, such as the mechanism of influence on the penetration barriers of the microbial cell (a mechanism characteristic of Pseudomonas aeruginosa) and the mechanism of efflux (active removal of an antimicrobial agent from the microbial cell), can also reduce the sensitivity of microorganisms to levofloxacin. Due to the specific mechanism of action of levofloxacin, there is usually no cross-resistance between levofloxacin and other antimicrobial agents. Clinical efficacy (efficacy in clinical trials in the treatment of infections caused by the following microorganisms):

Gram-positive aerobic microorganisms: Enterococcus faecalis, Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes.

Gram-negative Aerobic microorganisms: Citrobacter freundii, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella (Branhamella) catarrhalis, Morganella morganii, Proteus mirabilis, Pseudomonas aeruginosa, Serratia marcescens.

Others: Chlamydia pneumoniae, Legionella pneumophila, Mycoplasma pneumoniae.

PharmacokineticsAbsorption rate

Levofloxacin is rapidly and almost completely absorbed after oral use, food intake has little effect on its absorption. Absolute oral bioavailability is 99-100%. After a single dose of 500 mg of levofloxacin, the maximum plasma concentration (Cmax) is reached within 1-2 hours and is 5.2±1.2 mcg / ml. The pharmacokinetics of levofloxacin are linear in the dose range from 50 to 1000 mg. The equilibrium state of levofloxacin concentration in blood plasma when taking 500 mg of levofloxacin 1 or 2 times a day is reached within 48 hours.

On day 10 of oral use of Leflobact® 500 mg 1 time per day, the cmax of levofloxacin was 5.7±1.4 mcg / ml, and the minimum concentration of levofloxacin (concentration before the next dose) (Cmin) in blood plasma was 0.5±0.2 mcg/ml.

On day 10 of oral use of Leflobact® 500 mg 2 times a day, the Cmax was 7.8±1.1 mcg / ml, and the Cmin was 3.0±0.9 mcg/ml.

Distribution

The relationship with serum proteins is 30-40%. After a single and repeated use of 500 mg of levofloxacin, the volume of distribution of levofloxacin is, on average,100 liters, which indicates a good penetration of levofloxacin into the organs and tissues of the human body.

Penetration into the bronchial mucosa, epithelial lining fluid, alveolar macrophages

After a single oral dose of 500 mg of levofloxacin, the maximum concentrations of levofloxacin in the bronchial mucosa and epithelial lining fluid were reached within 1 h or 4 h and were 8.3 mcg/g and 10.8 mcg / ml, respectively, with penetration coefficients into the bronchial mucosa and epithelial lining fluid, compared with plasma concentrations of 1.1-1.8 and 0.8-3, respectively.

After 5 days of oral use of 500 mg of levofloxacin, the average concentrations of levofloxacin 4 hours after the last dose of the drug in the fluid of the epithelial lining were 9.94 mcg / ml and in alveolar macrophages – 97.9 mcg/ml.

Penetration of lung tissue

Maximum concentrations in the lung tissue after oral use of 500 mg of levofloxacin were approximately 11.3 mcg / g and reached 4-6 hours after taking the drug with penetration coefficients 2-5, compared with the concentration in blood plasma.

Penetration into the alveolar fluid

After 3 days of taking 500 mg of levofloxacin 1 or 2 times a day, the maximum concentrations of levofloxacin in the alveolar fluid were reached 2-4 hours after taking the drug and were 4.0 and 6.7 micrograms / ml, respectively, with a penetration coefficient of 1, compared with the concentration in blood plasma.

Bone penetration

Levofloxacin penetrates well into the cortical and spongy bone tissue, both in the proximal and distal femur, with a penetration coefficient (bone/blood plasma) of 0.1-3. The maximum concentrations of levofloxacin in the spongy bone tissue of the proximal femur after oral use of 500 mg of the drug were approximately 15.1 mcg/g (2 hours after taking the drug).

Penetration into the cerebrospinal fluid

Levofloxacin does not penetrate well into the cerebrospinal fluid.

Penetration of prostate tissue

After oral use of 500 mg of levofloxacin once a day for 3 days, the average concentration of levofloxacin in the prostate tissue was 8.7 mcg/g, the average ratio of prostate / blood plasma concentrations was 1.84.

Concentrations in the urine

Mean urinary concentrations 8-12 hours after oral doses of 150,300, and 600 mg of levofloxacin were 44 mcg / ml,91 mcg/ml, and 162 mcg / ml, respectively.

Metabolism

Levofloxacin is only slightly metabolized (5% of the dose taken). Its metabolites are demethylvofloxacin and levofloxacin N-oxide, which are excreted by the kidneys. Levofloxacin is stereochemically stable and does not undergo chiral transformations.

Deduction

After oral use, levofloxacin is relatively slowly eliminated from the blood plasma (half-life (T 1/2) – 6-8 hours). Excretion, mainly through the kidneys (more than 85% of the dose taken). The total clearance of levofloxacin after a single 500 mg dose was 175±29.2 ml/min.

There are no significant differences in the pharmacokinetics of levofloxacin when administered intravenously and when taken orally, which confirms that oral use and intravenous use are interchangeable.

Pharmacokinetics in individual groups of patients

, the pharmacokinetics of levofloxacin in men and women do not differ.

Pharmacokinetics in elderly patients do not differ from those in young patients, with the exception of pharmacokinetic differences associated with differences in creatinine clearance (CC).

In patients with renal insufficiency, the pharmacokinetics of levofloxacin are altered. As renal function worsens, renal excretion and renal clearance (CIR) decrease and T 1/2 increases.

Indications

Bacterial infections sensitive to levofloxacin in adults:

acute sinusitis;

exacerbation of chronic bronchitis;

community-acquired pneumonia;

uncomplicated urinary tract infections;

complicated urinary tract infections (including pyelonephritis);

chronic bacterial prostatitis;

skin and soft tissue infections;

for the complex treatment of drug-resistant forms of tuberculosis;

prevention and treatment of anthrax in the airborne route of infection.

When using Leflobact®, you should take into account the official national recommendations for the proper use of antibacterial drugs, as well as the sensitivity of pathogens in a particular country (see the section “Special instructions”).

Contraindications

hypersensitivity to levofloxacin, to other fluoroquinolones or to any other component of the drug;

epilepsy;

psevdoparalitichesky myasthenia gravis (myasthenia gravis) (see “Side effects”, the “Special instructions”);

lesions of the tendons at the earlier treatment quinolones;

the impairment of renal function (with CC less than 20 ml/min);

while on hemodialysis;

pregnancy (it is impossible to completely eliminate the risk of destruction of the cartilage growth points in the fetus);

breastfeeding (it is impossible to completely eliminate the risk of destruction of the cartilage of the growth points of the child);

childhood and adolescence to 18 years (due to the incomplete growth of the skeleton, as it is impossible to completely eliminate the risk of cartilage growth points);

lactase deficiency, lactose intolerance or glucose-galactose malabsorption.

With caution

In patients predisposed to the development of seizures (in patients with previous lesions of the central nervous system (CNS), in patients receiving concomitant medications that reduce the threshold of convulsive readiness of the brain, such as fenbufen, theophylline) (see the section “Interaction with other drugs”).

In patients with latent or manifest glucose-6-phosphate dehydrogenase deficiency (increased risk of hemolytic reactions during quinolone treatment).

In patients with impaired renal function with creatinine clearance of 20-50 ml / min (mandatory monitoring of renal function is required, as well as correction of the dosage regimen, see the section “Dosage and use”).

In patients with known risk factors for prolongation of the QT interval: in elderly patients; in female patients, in patients with uncorrected electrolyte disorders (hypokalemia, hypomagnesemia); with congenital prolongation of the QT interval syndrome; with heart diseases (heart failure, myocardial infarction, bradycardia); while taking medications that can prolong the QT interval (class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, neuroleptics) (see sections “Overdose”, “Interaction with other drugs”, “Special instructions”).

Patients with diabetes mellitus who receive oral hypoglycemic drugs, such as glibenclamide or insulin preparations (the risk of hypoglycemia increases).

In patients with severe adverse reactions to other fluoroquinolones, such as severe neurological reactions (increased risk of similar adverse reactions with levofloxacin).

In patients with psychosis or in patients with a history of mental illness (see section “Special instructions”).

Side effects

The following side effects are presented according to the following frequency gradations: very common (≥ 1/10); common (≥ 1/100, < 1/10); uncommon (≥ 1/1000, < 1/100); rare (≥ 1/10000, < 1/1000); very rare (

Cardiac disorders: rarely-sinus tachycardia, palpitation sensation; frequency unknown (post-marketing data) – prolongation of the QT interval, ventricular arrhythmias, ventricular tachycardia, ventricular tachycardia of the “pirouette” type, which can lead to cardiac arrest (see the sections “Overdose”, “Special instructions”).

Disorders of the blood and lymphatic system: infrequently – leukopenia (decrease in the number of white blood cells in the peripheral blood), eosinophilia (increase in the number of eosinophils in the peripheral blood); rarely – neutropenia (decrease in the number of neutrophils in the peripheral blood), thrombocytopenia (decrease in the number of platelets in the peripheral blood); frequency unknown (post – marketing data) – pancytopenia (decrease in the number of all shaped elements in the peripheral blood), agranulocytosis (absence or sharp decrease in the number of granulocytes in the peripheral blood), hemolytic anemia.

Nervous system disorders: often – headache, dizziness; infrequently – drowsiness, tremor, dysgeusia (taste distortion); rarely – paresthesia, convulsions (see section “Special instructions”); frequency unknown (post – marketing data)-peripheral sensory neuropathy, peripheral sensory-motor neuropathy (see section “Special instructions”), dyskinesia, extrapyramidal disorders, ageusia (loss of taste sensations), parosmia (odour disorder, especially a subjective sense of smell that is objectively absent), including loss of smell, fainting, benign intracranial hypertension.

Visual disturbances: rare-visual disturbances such as blurred vision; frequency unknown (post-marketing data) – transient vision loss, uveitis.

Hearing disorders and labyrinthine disorders: infrequently-vertigo (feeling of deviation or whirling or one’s own body or surrounding objects); rarely-tinnitus; frequency unknown (post-marketing data) – hearing loss, hearing loss.

Respiratory, thoracic and mediastinal disorders: infrequently-dyspnea; frequency unknown (post-marketing data) – bronchospasm, allergic pneumonitis.

Gastrointestinal disorders: often – diarrhea, vomiting, nausea; infrequently-abdominal pain, dyspepsia, flatulence, constipation; frequency unknown (post-marketing data) – hemorrhagic diarrhea, which in very rare cases can be a sign of enterocolitis, including pseudomembranous colitis (see section “Special instructions”), pancreatitis.

Renal and urinary tract disorders: infrequently-increased serum creatinine; rarely-acute renal failure (for example, due to the development of interstitial nephritis).

Skin and subcutaneous tissue disorders: infrequently-rash, pruritus, urticaria, hyperhidrosis; frequency unknown (post-marketing data) – toxic epidermal necrolysis, Stevens-Johnson syndrome, exudative erythema multiforme, photosensitization reactions (hypersensitivity to sunlight and ultraviolet radiation (see section “Special instructions”), leukocytoclastic vasculitis, stomatitis. Reactions from the skin and mucous membranes can sometimes develop even after taking the first dose of the drug.

Musculoskeletal and connective tissue disorders: infrequently-arthralgia, myalgia; rarely – tendon damage, including tendinitis (for example, Achilles tendon), muscle weakness, which can be particularly dangerous in patients with pseudoparalytic myasthenia gravis (see section “Special instructions”); frequency unknown (post – marketing data) – rhabdomyolysis, tendon rupture (for example, Achilles tendon rupture). tendons. This side effect may occur within 48 hours after starting treatment and may be bilateral in nature( see also the section “Special instructions”)), ligament rupture, muscle rupture, arthritis.

Metabolic and nutritional disorders: infrequently-anorexia; rarely-hypoglycemia, especially in patients with diabetes mellitus (possible signs of hypoglycemia: “wolfish” appetite, nervousness, perspiration, trembling); frequency unknown-hyperglycemia, hypoglycemic coma (see the section “Special instructions”).

Infectious and parasitic diseases: infrequently-fungal infections, development of resistance of pathogenic microorganisms.

Vascular disorders: rarely-a decrease in blood pressure. Common disorders: infrequently-asthenia; rarely-pyrexia (fever); frequency unknown-pain (including pain in the back, chest and extremities).

Immune system disorders: rarely-angioedema; frequency unknown (post-marketing data) – anaphylactic shock, anaphylactoid shock. Anaphylactic and anaphylactoid reactions can sometimes develop even after taking the first dose of the drug.

Liver and biliary tract disorders: often – increased activity of “liver” enzymes in the blood (for example, alanine aminotransferase (ALT), aspartate aminotransferase (AST)), increased activity of alkaline phosphatase (ALP) and gamma-glutamyltransferase (GGT); infrequently – increased concentration of bilirubin in the blood; frequency unknown (post – marketing data) – severe liver failure, including cases of acute liver failure insufficiency, sometimes fatal, especially in patients with a severe underlying disease (for example, in patients with sepsis) (see the section “Special instructions”), hepatitis, jaundice.

Mental disorders: often – insomnia; infrequently-feelings of anxiety, anxiety, confusion; rarely-mental disorders (for example, hallucinations, paranoia), depression, agitation (agitation), sleep disorders, nightmares; frequency unknown (post-marketing data) – mental disorders with behavioral disorders with self-harm, including suicidal thoughts and suicide attempts.

Other possible adverse effects related to all fluoroquinolones: very rare – attacks of porphyria (a very rare metabolic disease) in patients with porphyria.

Interaction

With preparations containing magnesium, aluminum, iron and zinc, didanosine

Preparations containing divalent or trivalent cations, such as zinc or iron salts (drugs for the treatment of anemia), magnesium – and/or aluminum-containing drugs (such as antacids), didanosine (only dosage forms containing aluminum or magnesium as a buffer), are recommended to be taken at least 2 hours before or 2 hours after taking Leflobact®tablets.

Calcium salts have a minimal effect on the absorption of levofloxacin when taken orally.

With sucralfate

The effect of the drug Leflobact® is significantly weakened with the simultaneous use of sucralfate (a means to protect the gastric mucosa). Patients receiving levofloxacin and sucralfate are advised to take sucralfate 2 hours after taking levofloxacin.

No pharmacokinetic interaction of levofloxacin with theophylline was detected with theophylline, fenbufen or similar drugs from the group of nonsteroidal anti-inflammatory drugs that reduce the threshold of convulsive readiness of the brain

. However, with the simultaneous use of quinolones and theophylline, nonsteroidal anti-inflammatory drugs and other drugs that reduce the threshold of convulsive readiness of the brain, a pronounced decrease in the threshold of convulsive readiness of the brain is possible.

The concentration of levofloxacin with simultaneous use of fenbufen increases only by 13%.

With indirect anticoagulants (vitamin K antagonists)

Patients treated with levofloxacin in combination with indirect anticoagulants (for example, warfarin) experienced an increase in prothrombin time/international normalized ratio and/or the development of bleeding, including severe bleeding. Therefore, with the simultaneous use of indirect anticoagulants and levofloxacin, regular monitoring of blood clotting parameters is necessary.

With probenecid and cimetidine

Caution should be exercised when concomitantly using medications that interfere with renal tubular secretion, such as probenecid and cimetidine, and levofloxacin, especially in patients with renal insufficiency.

Elimination (renal clearance)of levofloxacin is slowed by cimetidine by 24% and probenecid by 34%. It is unlikely that this can be of clinical significance in normal renal function.

With cyclosporine

Levofloxacin increased the half-life of cyclosporine by 33%. Since this increase is clinically insignificant, no dose adjustment of cyclosporine is required when it is co-administered with levofloxacin.

With glucocorticosteroids

Concomitant use of glucocorticosteroids increases the risk of tendon rupture.

With medications that extend the QT interval

Levofloxacin, like other fluoroquinolones, should be used with caution in patients receiving drugs that prolong the QT interval (for example, Class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, neuroleptics).

Other services

Clinical and pharmacological studies conducted to study possible pharmacokinetic interactions of levofloxacin with digoxin, glibenclamide, ranitidine and warfarin have shown that the pharmacokinetics of levofloxacin when used concomitantly with these drugs do not change sufficiently to have clinical significance.

How to take, course of use and dosage

Inside, before meals or in between meals, without chewing, with a sufficient amount of liquid (from 0.5 to 1 cup).

The drug should be taken at least 2 hours before or 2 hours after taking medications containing magnesium and / or aluminum, iron, zinc, or sucralfate.

If you accidentally miss taking the drug, you should take the next dose as soon as possible and continue taking Leflobact® according to the recommended dosage regimen.

Acute sinusitis-500 mg once a day, for 10-14 days.

Exacerbation of chronic bronchitis-500 mg 1 time a day, for 7-10 days.

Community-acquired pneumonia-500 mg 1-2 times a day, for 7-14 days.

Uncomplicated urinary tract infections-250 mg 1 time a day, for 3 days.

Complicated urinary tract infections-500 mg once a day, for 7-14 days.

Pyelonephritis – 500 mg once a day, for 7-10 days.

Chronic bacterial prostatitis – 500 mg once a day, for 28 days.

Infections of the skin and soft tissues – 500 mg 1-2 times a day, for 7-14 days.

Comprehensive treatment of drug-resistant forms of tuberculosis-500 mg 1-2 times a day-up to 3 months.

Prevention and treatment of anthrax with airborne infection-500 mg 1 time a day-up to 8 weeks.

Levofloxacin is mainly excreted through the kidneys, so when treating patients with limited renal function, it is necessary to reduce the dose of the drug.

It is possible to prescribe the drug Leflobact® in tablets to continue the course of treatment for those patients who were first prescribed intravenous use of the drug Leflobact® solution for infusions and their condition improved, allowing for further oral use of levofloxacin.

Dosage regimen in patients with impaired liver function

If liver function is impaired, no dosage adjustment is required, since levofloxacin is only slightly metabolized in the liver.

Dosage regimen in elderly patients.

Elderly patients do not need to adjust the dosage regimen, except in cases where creatinine clearance decreases to 50 ml/min or lower.

Overdose

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

Special instructions

The use of the drug during pregnancy is contraindicated. When prescribing the drug during lactation, you should decide whether to stop breastfeeding.

Hospital infections caused by Pseudomonas aeruginosa (Pseudomonas aeruginosa) may require combined treatment.

The prevalence of acquired resistance of the seeded strains of microorganisms may vary depending on the geographical region and over time. Therefore, information on drug resistance in a particular country is required. For the treatment of severe infections or if treatment is ineffective, a microbiological diagnosis should be established with the isolation of the pathogen and determination of its sensitivity to levofloxacin.

Methicillin-resistant Staphylococcus aureus

There is a high probability that methicillin-resistant Staphylococcus aureus will be resistant to fluoroquinolones, including levofloxacin. Therefore, levofloxacin is not recommended for the treatment of established or suspected infections caused by methicillin-resistant Staphylococcus aureus, if laboratory tests have not confirmed the sensitivity of this microorganism to levofloxacin.

Patients predisposed to developing seizures

Like other quinolones, levofloxacin should be used with great caution in patients with a predisposition to seizures. These patients include patients with previous central nervous system disorders, such as stroke, severe traumatic brain injury; patients receiving concomitant medications that lower the threshold for brain seizure readiness, such as fenbufen and other similar nonsteroidal anti-inflammatory drugs or other drugs that lower the threshold for seizure readiness, such as theophylline ) (see the section “Interaction with other medications”).

Pseudomembranous colitis

Diarrhea that develops during or after treatment with levofloxacin, especially severe, persistent and/or bloody, may be a symptom of pseudomembranous colitis caused by Clostridium difficile. If pseudomembranous colitis is suspected, treatment with levofloxacin should be stopped immediately and specific antibiotic therapy (vancomycin, teicoplanin or metronidazole orally) should be initiated immediately. Drugs that inhibit intestinal motility are contraindicated.

Tendinitis

Rarely observed tendinitis with quinolones, including levofloxacin, can lead to tendon rupture, including the Achilles tendon. This side effect may develop within 48 hours of starting treatment and may be bilateral. Elderly patients are more likely to develop tendinitis. The risk of tendon rupture may increase with concomitant use of corticosteroids. If tendinitis is suspected, immediately discontinue treatment with Leflobact® and start appropriate treatment of the affected tendon, for example, by ensuring that it is sufficiently immobilized (see sections “Contraindications” and “Side effects”).

Hypersensitivity reactions

Levofloxacin can cause serious, potentially fatal, hypersensitivity reactions (angioedema, anaphylactic shock), even with the use of initial doses (see the section “Side effects”). Patients should immediately stop taking the drug and consult a doctor.

Severe bullous reactions

Severe bullous skin reactions, such as Stevens-Johnson syndrome or toxic epidermal necrolysis, have been reported with levofloxacin (see section “Side effects”). In case of any skin or mucosal reactions, the patient should immediately consult a doctor and not continue treatment until after consultation.

Liver and biliary tract disorders

Cases of hepatic necrosis, including fatal liver failure, have been reported with levofloxacin, mainly in patients with severe underlying medical conditions, such as sepsis (see section “Adverse effects”). Patients should be warned to stop treatment and seek immediate medical attention if signs and symptoms of liver damage appear, such as anorexia, jaundice, dark urine, itching, and abdominal pain.

Patients with renal insufficiency

Since levofloxacin is mainly excreted through the kidneys, patients with impaired renal function require mandatory monitoring of renal function, as well as correction of the dosage regimen (see the section “Dosage and use”). When treating elderly patients, it should be borne in mind that patients in this group often have impaired renal function (see the section “Dosage and use”).

Prevention of photosensitization reactions

Although photosensitization with levofloxacin is very rare, to prevent its development, patients are not recommended to be exposed to strong solar or artificial ultraviolet radiation (for example, to visit a tanning salon) during treatment and within 48 hours after the end of treatment with levofloxacin.

Superinfection

As with other antibiotics, the use of levofloxacin, especially for a long time, can lead to increased reproduction of microorganisms that are insensitive to it (bacteria and fungi), which can cause changes in the microflora that is normally present in humans. As a result, superinfection may develop. Therefore, it is mandatory to re-evaluate the patient’s condition during treatment, and if superinfection develops during treatment, appropriate measures should be taken.

Prolongation of the QT interval

Very rare cases of QT prolongation have been reported in patients taking fluoroquinolones, including levofloxacin.

Caution should be exercised when using fluoroquinolones, including levofloxacin, in patients with known risk factors for prolongation of the QT interval: in patients with uncorrected electrolyte disturbances (hypokalemia, hypomagnesemia); with congenital QT prolongation syndrome; with heart diseases (heart failure, myocardial infarction, bradycardia); while taking medications that can prolong the QT interval, such as class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, antipsychotics. Elderly and female patients may be more sensitive to drugs that prolong the QT interval. Therefore, fluoroquinolones, including levofloxacin, should be used with caution (see sections “With caution”, “Dosage and use”, “Side effects”, “Interaction with other drugs”). Patients with glucose-6-phosphate dehydrogenase deficiency

Patients with latent or manifest glucose-6-phosphate dehydrogenase deficiency have a predisposition to hemolytic reactions when treated with quinolones, which should be taken into account when treated with levofloxacin.

Hypo – and hyperglycemia (dysglycemia)

As with other quinolones, hypoglycaemia and hyperglycaemia have been reported with levofloxacin, usually in patients with diabetes mellitus receiving concomitant treatment with oral hypoglycaemic drugs (e. g., glibenclamide) or insulin preparations. Cases of hypoglycemic coma have been reported. In patients with diabetes mellitus, monitoring of blood glucose concentration is required (see the section “Side effects”).

Peripheral neuropathy

Patients taking fluoroquinolones, including levofloxacin, have experienced sensory and sensorimotor peripheral neuropathy, which may start quickly. If the patient develops symptoms of neuropathy, levofloxacin should be discontinued. This minimizes the possible risk of irreversible changes.

Exacerbation of pseudoparalytic myasthenia gravis

Fluoroquinolones, including levofloxacin, are characterized by neuromuscular blocking activity and may increase muscle weakness in patients with pseudoparalytic myasthenia gravis. In the post-marketing period, adverse reactions were observed, including pulmonary insufficiency that required mechanical ventilation, and death, which were associated with the use of fluoroquinolones in patients with pseudoparalytic myasthenia gravis. The use of levofloxacin in a patient with an established diagnosis of pseudoparalytic myasthenia gravis is not recommended (see the section “Side effects”).

Application in the airborne pathway of anthrax infection

The use of levofloxacin in humans for this indication is based on data on the sensitivity of Bacillus anthracis to it, obtained in vitro studies and in experimental studies conducted on animals, as well as on limited data on the use of levofloxacin in humans. Treating physicians should refer to national and / or international documents that reflect a common point of view on the treatment of anthrax.

Psychotic reactions

Psychotic reactions have been reported with the use of quinolones, including levofloxacin, which in very rare cases progressed to the development of suicidal thoughts and behavioral disorders with self-harm (sometimes after taking a single dose of levofloxacin (see section “Side effects”)). If such reactions develop, treatment with levofloxacin should be discontinued and appropriate therapy should be prescribed. Caution should be exercised when prescribing the drug to patients with psychosis or a history of mental illness.

Visual disturbances

If you develop any visual disturbances, you should immediately consult an ophthalmologist (see the section “Side effects”).

Impact on laboratory tests

In patients taking levofloxacin, the determination of opiates in the urine may lead to false positive results, which should be confirmed by more specific methods.

Levofloxacin can inhibit the growth of Mycobacterium tuberculosis and subsequently lead to false negative results of the bacteriological diagnosis of tuberculosis.

Influence on the ability to drive vehicles and mechanisms

Side effects of Leflobact ®, such as dizziness or vertigo, drowsiness and visual disturbances (see the section “Side effects”), may reduce psychomotor reactions and the ability to concentrate. This can pose a certain risk in situations where these abilities are particularly important (for example, when driving a car, when servicing machines and mechanisms, when performing work in an unstable position).

Form of production

Tablets with a dosage of 500 mg are oval, covered with a yellow film coating. 10 pcs. in the package.

Storage conditions

In a place protected from light at a temperature not exceeding 25 ° C. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Levofloxacin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor

Indications

Sinusitis, Skin Infections, Respiratory Tract Infections, Sinusitis, Urinary Tract Infections, Pneumonia, Tuberculosis, Bronchitis, Prostatitis, Infectious Diseases, Boils, Inflammation of the female genital organs