Leflobact Forte pills 750mg, 10pcs

Composition

Per tablet:

Core composition:

Active ingredient:  levofloxacin hemihydrate – 768.69 mg (in terms of levofloxacin-750 mg);

Auxiliary substances:  calcium stearate, pre-gelatinized starch (starch 1500), crospovidone (collidone CL-M, collidone CL), povidone (polyvinylpyrrolidone low molecular weight medical 12600±2700, povidone K 15, povidone K 17), lactose monohydrate (milk sugar), talc, microcrystalline cellulose, potato starch;

Shell composition:  hypromellose (hydroxy-propylmethylcellulose), macrogol-4000 (polyethylene glycol-4000), titanium dioxide (titanium dioxide), tropeolin O.

Pharmacological action

Pharmacotherapy group: Antimicrobial agent-fluoroquinolonate:  

J. 01. M. A Fluoroquinolones

J. 01. M. A. 12 Levofloxacin

Pharmacodynamics : Leflobact ® FORTE is a synthetic broad-spectrum antimicrobial bactericidal drug from the group of fluoroquinolones containing levofloxacin, the levorotatory isomer of ofloxacin, as the Active ingredient.

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 vitro

Sensitive microorganisms (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).

– Gram-negative aerobic 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 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), Morganella morganii, Neisseria gonorrhoeae non-PPNG/PPNG (reproducirse and producing penicillinase), 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), 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.

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.

Resistance

Resistance 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. Pharmacokinetics:

Suction

When taken orally, it is rapidly and almost completely absorbed (food intake has little effect on the speed and completeness of absorption). Bioavailability – 99%. The time required to reach the maximum concentration (Cmax) is 1-2 hours. The maximum concentration (Cmax) in plasma is 8.0 mcg / ml.

Distribution

The equilibrium concentration in the blood plasma is reached within 48 hours. The relationship with serum 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, cerebrospinal fluid, polymorphonuclear leukocytes, alveolar macrophages.

Metabolism

Levofloxacin undergoes limited liver metabolism (oxidation and / or deacetylation). 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). It is excreted mainly by the kidneys (by glomerular filtration and tubular secretion). Renal clearance is 70% of the total clearance. Less than 5% of levofloxacin is excreted as metabolites. After oral use in unchanged form,70% of the dose is excreted by the kidneys within 24 hours and 87% by 48 hours; 4% of the oral dose is excreted by the intestines within 72 hours

. 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 clearance (SIR) decrease and T 1/2 increases.

Indications

Infectious and inflammatory diseases caused by levofloxacin-sensitive microorganisms in adults:

– lower respiratory tract infections (hospital-acquired pneumonia, community-acquired pneumonia);

– acute bacterial sinusitis;

– complicated urinary tract infections (including acute pyelonephritis);

– complicated skin and soft tissue infections (including suppurated atheromas, abscess, furunculosis).

When using Leflobact® FORTE, you should take into account the official national guidelines for the proper use of antibacterial drugs, as well as the sensitivity of pathogens in a particular country.

Use during pregnancy and lactation

Pregnancy

The use of the drug during pregnancy is contraindicated.

Lactation period

When prescribing the drug during lactation, you should decide whether to stop breastfeeding.

Contraindications

-Hypersensitivity to levofloxacin, other fluoroquinolones or any other component of the drug.

– Epilepsy.

– Pseudoparalytic myasthenia gravis.

– A history of tendon damage when taking fluoroquinolones.

– Pregnancy (the risk of damage to cartilage growth points in the fetus cannot be completely excluded).

– The period of breastfeeding (theClinical 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

The drug should be taken orally before meals or in between meals, without chewing, with a sufficient amount of liquid (from 0.5 to 1 cup).

Adult patients with normal renal function (creatinine clearance greater than 50 ml/min) should be administered according to the regimens shown in the table:

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

For patients with impaired renal function (creatinine clearance < 50 ml/min), other doses of levofloxacin should be used.

No additional doses are required after hemodialysis or permanent outpatient peritoneal dialysis (PAPD).

If liver function is impaired, no dose adjustment is required, since the volume of levofloxacin metabolism in the liver is limited.

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 gastrointestinal mucosa, prolongation of the QT interval, confusion, dizziness, convulsions, hallucinations, tremor.

Treatment: symptomatic, gastric lavage and use of antacids to protect the gastric mucosa, dialysis is ineffective. There is no specific antidote.

Special instructions

After normalization of body temperature, it is recommended to continue treatment for at least 48-72 hours.

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.

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 convulsive readiness of the brain, such as fenbufen and other similar nonsteroidal anti-inflammatory drugs or other drugs that lower the threshold for convulsive readiness, such as theophylline.

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, treatment with levofloxacin should be stopped immediately and appropriate treatment should be initiated for the affected tendon, for example, by ensuring that it is sufficiently immobilized.

Hypersensitivity reactions

Levofloxacin can cause serious, potentially fatal, hypersensitivity reactions (angioedema, anaphylactic shock), even with the use of initial doses. 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. 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

Hepatic necrosis, including fatal liver failure, has been reported with levofloxacin, mainly in patients with severe underlying medical conditions, such as sepsis.

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, in patients with impaired renal function (CC When treating elderly patients, it should be borne in mind that patients in this group often have impaired renal function.

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 UV radiation (for example, to visit a tanning salon) during treatment and within 48 hours after the end of treatment with levofloxacin. If phototoxicity develops, treatment with the drug should be discontinued.

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.

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. Blood glucose monitoring is required in patients with diabetes mellitus.

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.

Adverse reactions have been reported, including pulmonary insufficiency that required mechanical ventilation and death, which have been 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.

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). 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 may inhibit growth Mycobacterium tuberculosis and lead in the future to false negative results of the bacteriological diagnosis of tuberculosis. Influence on the ability to drive vehicles and mechanisms:

Side effects of Leflobact FORTE, such as dizziness or vertigo, drowsiness and visual disturbances (see 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).

Storage conditions

Store in a dark place at a temperature not exceeding 25 °C.

Keep out of the 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