Hyleflox, 5 pcs., 500 mg, film-coated tablets

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Synthetic fluoroquinolone , which has a wide spectrum of action. The mechanism of action is due to inhibition of DNA gyrase (responsible for DNA biosynthesis and replication ) and topoisomerase IV , disruption of DNA , suppression of its synthesis, and induction of profound changes in the cytoplasm and membrane of microorganisms. Effective against aerobic , anaerobic , as well as other microorganisms ( bartonella , chlamydia , mycobacterium tuberculosis , legionella , mycoplasma and ureaplasma ).

Pharmacokinetics

After administration, it is quickly absorbed from the gastrointestinal tract . Cmax in the blood is determined after 1–2 hours, and the equilibrium concentration after 48 hours. Bioavailability is 99%. Binds to proteins by 30%. Penetrates well into the lungs, sputum, bronchial mucosa, and organs of the genitourinary system.

Metabolized in the liver. It is excreted mostly by the kidneys: 70% unchanged in 24 hours. A small part of the dose is excreted by the intestines. T1/2 - 7-8 hours.

Description

Capsule-shaped biconvex tablets, film-coated, white or almost white; on the cross section two layers are visible, the inner layer is light yellow to yellow in color, white inclusions are allowed.

Pharmacotherapeutic group:

antimicrobial agent, fluoroquinolone.

ATX code:

J01MA12.

Pharmacological properties

Pharmacodynamics

Levofloxacin is a synthetic broad-spectrum antibacterial drug from the group of fluoroquinolones, containing the levorotatory isomer of ofloxacin as an active substance.

Levofloxacin blocks DNA gyrase, disrupts supercoiling and cross-linking of DNA breaks, inhibits DNA synthesis, and causes profound morphological changes in the cytoplasm, cell wall and membranes of bacteria.

Levofloxacin has a bactericidal effect and is active against a large number of pathogens of bacterial infections both in vitro

, and
in vivo
.

Sensitive microorganisms (minimum inhibitory concentration (MIC) ≤ 2 mg/l):

• aerobic gram-positive microorganisms: Bacillus anthracis , Corynebacterium diphtheriae , Corynebacterium jeikeium , Enterococcus spp
  ., including
  Enterococcus faecalis, Listeria monocytogenes, Staphylococcus spp.
  ( coagulase-negative, methicillin-sensitive/leukotoxin-containing/moderately sensitive strains), including
  Staphylococcus aureus (
  methicillin-sensitive strains
  ), Staphylococcus epidermidis (
  methicillin-sensitive strains
  ), Streptococcus spp.
  groups C and G, Streptococcus agalactiae, Streptococcus pneumoniae ( penicillin-sensitive / moderately sensitive / resistant strains
  ), Streptococcus pyogenes, Streptococcus spp.
  Viridans group ( penicillin-sensitive/resistant strains
  );
• aerobic gram-negative microorganisms: Acinetobacter spp .
  , including
  Acinetobacter baumannii , Acinetobacillus actinomycetemcomitans , Citrobacter freundii , Eikenella corrodens , Enterobacter spp
  ., including
  Enterobacter aerogenes , Enterobacter cloacae , Escherichia coli , Gardnerella vaginalis , Haemophilus ducreyi , Haemophilus influenzae
  (ampicillin-sensitive/ resistant strains),
  Haemophilus parainfluenzae , Helicobacter pylori , Klebsiella spp
  ., including
  Klebsiella oxytoca , Klebsiella pneumoniae , Moraxella catarrhalis
  (beta-lactamase producing and non-producing strains),
  Morganella morganii , Neisseria gonorrhoeae
  (penicillinase producing and non-producing 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
  (hospital infections caused by
  Pseudomonas aeruginosa
  may require combination treatment),
  Serratia spp
  ., including
  Serratia marcescens , Salmonella spp
  .;
• 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 pneumophila , Legionella spp ., Mycobacterium spp .
  , including
  Mycobacterium leprae , Mycobacterium tuberculosis , Mycoplasma hominis , Mycoplasma pneumoniae , Rickettsia spp ., Ureaplasma urealyticum
  .

Moderately sensitive microorganisms (MIC = 4 mg/l):

• aerobic gram-positive microorganisms: Corynebacterium urealyticum , Corynebacterium xerosis , Enterococcus faecium , Staphylococcus epidermidis
  (methicillin-resistant strains),
  Staphylococcus haemolyticus
  (methicillin-resistant strains);
• aerobic gram-negative microorganisms: Campylobacter jejuni , Campylobacter coli
  ;
• anaerobic microorganisms: Prevotella spp ., Porphyromonas spp
  .

Resistant microorganisms (MIC more than 8 mg/l):

• aerobic gram-positive microorganisms: Staphylococcus aureus
  (methicillin-resistant strains), other
  Staphylococcus spp
  . (coagulase-negative methicillin-resistant strains);
• aerobic gram-negative microorganisms: Alcaligenes xylosoxidans
  ;
• anaerobic microorganisms: Bacteroides thetaiotaomicron
• other microorganisms: Mycobacterium avium
  .

Clinical efficacy (effectiveness in clinical studies against infections caused by the following microorganisms):

• aerobic gram-positive microorganisms: Enterococcus faecalis , Staphylococcus aureus , Streptococcus pneumoniae , Streptococcus pyogenes
  ;
• aerobic gram-negative microorganisms: Citrobacter freundii , Enterobacter cloacae , Escherichia coli , Haemophilus influenzae , Haemophilus parainfluenzae , Klebsiella pneumoniae , Moraxella catarrhalis , Morganella morganii , Proteus mirabilis , Pseudomonas aeruginosa , Serratia marcescens
  ;
• other microorganisms: Chlamydia pneumoniae , Legionella pneumophila , Mycoplasma pneumoniae
  .

Resistance to levofloxacin develops as a result of a stepwise process of mutations in the genes encoding both type II topoisomerases: DNA gyrase and topoisomerase IV. Other resistance mechanisms, such as the mechanism of influencing the penetration barriers of the microbial cell (a mechanism characteristic of Pseudomonas
aeruginosa
) and the mechanism of efflux (active removal of the antimicrobial agent from the microbial cell), may also reduce the sensitivity of microorganisms to levofloxacin.

Due to the peculiarities of the mechanism of action of levofloxacin, cross-resistance between levofloxacin and other antimicrobial agents is not usually observed.

Farmakok u no u ka

Absorption

Levofloxacin is rapidly and almost completely absorbed after oral administration; food intake has little effect on its absorption. Absolute bioavailability when taken orally is 99-100%. After a single dose of 500 mg of levofloxacin, the maximum concentration in blood plasma (Cmax) is reached within 1-2 hours and is 5.2 ± 1.2 μg/ml. The pharmacokinetics of levofloxacin is 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 achieved within 48 hours.

On the 10th day of oral administration of the drug Levofloxacin Ecolevid® 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 taking the next dose) (Cmin) in the blood plasma was 0.5 ±0.2 µg/ml.

On the 10th day of oral administration of the drug Levofloxacin Ecolevid® 500 mg 2 times a day, Cmax was 7.8 ± 1.1 μg/ml, and C min was 3.0 ± 0.9 μg/ml.

Distribution

The connection with serum proteins is 30-40%. After a single and repeated dose of 500 mg of levofloxacin, the volume of distribution of levofloxacin is, on average, 100 l, which indicates good penetration of levofloxacin into 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 hour or 4 hours and were 8.3 μg/g and 10.8 μg/ml, respectively, with penetration coefficients into the mucosa bronchi and epithelial lining fluid, compared with plasma concentrations of 1.1-1.8 and 0.8-3, respectively.

After 5 days of oral administration of 500 mg levofloxacin, the mean concentrations of levofloxacin 4 hours after the last dose in the epithelial lining fluid were 9.94 μg/ml and in alveolar macrophages - 97.9 μg/ml.

Penetration into lung tissue

Maximum concentrations in lung tissue after oral administration of 500 mg of levofloxacin were approximately 11.3 mcg/g and were achieved 4-6 hours after dosing with penetration coefficients of 2-5, compared with plasma concentrations.

Penetration into 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 μg/ml, respectively, with a penetration coefficient of 1. compared to plasma concentrations.

Penetration into bone tissue

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

Penetration into the cerebrospinal fluid

Levofloxacin penetrates poorly into the cerebrospinal fluid.

Penetration into prostate tissue

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

Concentrations in urine

Mean urinary concentrations 8 to 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 metabolized to a small extent (5% of the dose taken). Its metabolites are demethyllevofloxacin and levofloxacin N-oxide, which are excreted by the kidneys. Levofloxacin is stereochemically stable and does not undergo chiral transformations.

Removal

After oral administration, levofloxacin is relatively slowly eliminated from the blood plasma (half-life (T1/2) - 6-8 hours). Excretion is mainly through the kidneys (more than 85% of the dose taken). The total clearance of levofloxacin after a single dose of 500 mg was 175±29.2 ml/min.

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

Pharmacokinetics in selected patient groups

The pharmacokinetics of levofloxacin do not differ between men and women.

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

In renal failure, the pharmacokinetics of levofloxacin changes. As renal function deteriorates, renal excretion and renal clearance (CIR) decrease and T1/2 increases.

Pharmacokinetics in renal failure after a single oral dose of 500 mg of Levofloxacin Ecolevid®.

Side effects

• tremor , anxiety , headache , weakness, dizziness , insomnia or drowsiness , paresthesia, hallucinations , depression , convulsions;
• impaired hearing and vision, taste and tactile sensitivity;
• decreased blood pressure , tachycardia , atrial fibrillation ;
• nausea, diarrhea , loss of appetite, pseudomembranous colitis , abdominal pain;
• increased bilirubin , hepatitis ;
• hypoglycemia;
• muscle weakness, arthralgia , muscle pain, tendon rupture;
• interstitial nephritis;
• eosinophilia , leukopenia , agranulocytosis , neutropenia , pancytopenia , thrombocytopenia , hemorrhages ;
• skin itching, urticaria , skin edema, Stevens-Johnson syndrome , bronchospasm , pneumonitis , anaphylactic shock , vasculitis ;
• asthenia , fever .

Hyleflox (Levofloxacin) TB p/o captivity 500 mg N 5

Active substance

levofloxacin

ATX code

J01MA12 (Levofloxacin)

Release form, packaging and composition of the drug

Film-coated tablets

light orange to orange in color, round, biconvex; at the break - the core is from white with a yellow tint to yellow.

[PRING] corn starch, microcrystalline cellulose, povidone K30, methyl parahydroxybenzoate, propyl parahydroxybenzoate, purified talc, magnesium stearate, sodium carboxymethyl starch.

Film shell composition:

hypromellose, purified talc, macrogol 6000, titanium dioxide, sunset yellow dye.

3 pcs. - blisters (1) - cardboard packs. 3 pcs. - blisters (10) - cardboard packs. 5 pieces. - blisters (1) - cardboard packs. 5 pieces. - blisters (2) - cardboard packs. 5 pieces. - blisters (10) - cardboard packs. 10 pieces. - blisters (1) - cardboard packs. 10 pieces. - blisters (10) - cardboard packs. 100 pieces. — polymer bags (1) — plastic jars. 500 pcs. — polymer bags (1) — plastic jars. 1000 pcs. — polymer bags (1) — plastic jars.

Film-coated tablets

light orange to orange in color, oval, biconvex, with a notch on one side; at the break - the core is from white with a yellow tint to yellow.

[PRING] corn starch, microcrystalline cellulose, povidone K30, methyl parahydroxybenzoate, propyl parahydroxybenzoate, purified talc, magnesium stearate, sodium carboxymethyl starch.

Film shell composition:

hypromellose, purified talc, macrogol 6000, titanium dioxide, sunset yellow dye.

5 pieces. - blisters (1) - cardboard packs. 5 pieces. - blisters (10) - cardboard packs. 10 pieces. - blisters (1) - cardboard packs. 10 pieces. - blisters (10) - cardboard packs. 100 pieces. — polymer bags (1) — plastic jars. 500 pcs. — polymer bags (1) — plastic jars. 1000 pcs. — polymer bags (1) — plastic jars.

Film-coated tablets

light orange to orange in color, oval, biconvex, with a notch on one side; at the break - the core is from white with a yellow tint to yellow.

[PRING] corn starch, microcrystalline cellulose, povidone K30, methyl parahydroxybenzoate, propyl parahydroxybenzoate, purified talc, magnesium stearate, sodium carboxymethyl starch.

Film shell composition:

hypromellose, purified talc, macrogol 6000, titanium dioxide, sunset yellow dye.

5 pieces. - blisters (1) - cardboard packs. 5 pieces. - blisters (10) - cardboard packs. 10 pieces. - blisters (1) - cardboard packs. 10 pieces. - blisters (10) - cardboard packs. 100 pieces. — polymer bags (1) — plastic jars. 500 pcs. — polymer bags (1) — plastic jars. 1000 pcs. — polymer bags (1) — plastic jars.

Clinical and pharmacological group

Antibacterial drug of the fluoroquinolone group

Pharmacotherapeutic group

Antimicrobial agent - fluoroquinolone

pharmachologic effect

Suction

After oral administration, levofloxacin is rapidly and almost completely absorbed from the gastrointestinal tract. Food intake has little effect on the speed and completeness of absorption. Bioavailability – 99%. Cmax in plasma is achieved after 1-2 hours and for levofloxacin in doses of 250 mg, 500 and 750 mg is 2.8 mcg/ml, 5.2 mcg/ml and 8 mcg/ml, respectively.

Distribution

After taking a single or multiple dose, the amount of absorbed drug is directly proportional to the dose taken. Css in plasma is achieved after 48 hours. The average Vd of levofloxacin varies from 74 to 112 l. Plasma protein binding 30-40%. Penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, alveolar macrophages (the concentration in lung tissue is 2-5 times higher than the concentration in plasma), organs of the genitourinary system, polymorphonuclear leukocytes.

Metabolism

Levofloxacin undergoes limited metabolism in the liver (oxidation and/or deacetylation).

Removal

It is excreted from the body primarily by the kidneys by glomerular filtration and tubular secretion. T1/2 of levofloxacin is 6-8 hours. Less than 5% of the dose taken is excreted in the form of desmethyl and N-oxide metabolites. Unchanged, 70% of the dose taken orally is excreted by the kidneys within 24 hours and 87% within 48 hours. 4% of the dose taken orally is excreted by the intestines within 72 hours.

Indications for use

Infectious and inflammatory diseases of mild to moderate severity caused by microorganisms sensitive to the drug:

• lower respiratory tract infections (pneumonia, exacerbation of chronic bronchitis);
• acute bacterial sinusitis;
• urinary tract and kidney infections (including acute pyelonephritis);
• infections of the skin and soft tissues (festering atheromas, abscess, boils);
• chronic bacterial prostatitis;
• intra-abdominal infection (in combination with antibacterial drugs acting on anaerobic microflora);
• tuberculosis (as part of complex therapy for drug-resistant forms).

Dosage

Orally, before meals or between meals, without chewing, with a sufficient amount of water.

Adult patients with normal renal function (creatinine clearance > 50 ml/min)

apply in accordance with the schemes presented in the table:

* This regimen is indicated for the treatment of community-acquired pneumonia caused by Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Mycoplasma pneumoniae, Chlamydia pneumoniae.

** This regimen is indicated for the treatment of urinary tract infections caused by Enterococcus faecalis, Enterococcus cloacae, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa and acute pyelonephritis caused by Escherichia coli.

*** This regimen is indicated for the treatment of urinary tract infections caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and acute pyelonephritis caused by Escherichia coli, including cases with concomitant bacteremia.

Dose adjustment of levofloxacin in adult patients with impaired renal function (creatinine clearance <50 ml/min).

In case of liver dysfunction

no dose adjustment is required, because The amount of metabolism of levofloxacin in the liver is limited.

Contraindications

• epilepsy;
• tendon damage associated with a history of quinolone use;
• children and adolescents up to 18 years of age;
• pregnancy;
• lactation period;
• history of hypersensitivity to levofoxacin, other fluoroquinolones or other components of the drug.

Carefully _

the drug should be prescribed to elderly patients (high probability of concomitant decline in renal function), with deficiency of glucose-6-phosphate dehydrogenase.

Overdose

Symptoms:

nausea, erosive lesions of the gastrointestinal mucous membranes, prolongation of the QT interval, confusion, dizziness, convulsions.

Treatment:

gastric lavage, if necessary - symptomatic therapy. There is no specific antidote, dialysis is ineffective.

Side effects

From the nervous system:

headache, dizziness, weakness, drowsiness, insomnia, tremor, anxiety, paresthesia, fear, hallucinations, confusion, depression, movement disorders, convulsions.

From the senses:

disturbances of vision, hearing, smell, taste and tactile sensitivity.

From the cardiovascular system:

decreased blood pressure, vascular collapse, tachycardia, prolongation of the QT interval, atrial fibrillation.

From the digestive system:

nausea, vomiting, diarrhea (including blood), indigestion, loss of appetite, abdominal pain, pseudomembranous colitis; increased activity of liver transaminases, hyperbilirubinemia, hepatitis, dysbacteriosis.

From the side of metabolism:

hypoglycemia (increased appetite, increased sweating, trembling, nervousness).

From the musculoskeletal system:

arthralgia, muscle weakness, myalgia, rhabdomyolysis, tendon rupture, tendinitis.

From the urinary system:

hypercreatininemia, interstitial nephritis, acute renal failure.

From the hematopoietic organs:

eosinophilia, hemolytic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhages.

Allergic reactions:

itching and hyperemia of the skin, swelling of the skin and mucous membranes, urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), bronchospasm, suffocation, anaphylactic shock, allergic pneumonitis, vasculitis.

Other:

photosensitivity, asthenia, exacerbation of porphyria, persistent fever, development of superinfection.

Overdose

Levofloxacin increases T1/2 of cyclosporine.

The effect of levofloxacin is reduced by drugs that inhibit intestinal motility, sucralfate, aluminum- or magnesium-containing antacid drugs and iron preparations.

NSAIDs and theophylline, when used simultaneously with levofloxacin, increase the risk of developing seizures in predisposed patients, and corticosteroids increase the risk of tendon rupture.

When levofloxacin is taken concomitantly with hypoglycemic agents, changes in blood glucose levels, including hyperglycemia and hypoglycemia, are possible.

Levofloxacin enhances the effect of warfarin.

Cimetidine and drugs that block tubular secretion slow down the elimination of levofloxacin.

Storage conditions

The drug should be stored out of the reach of children, in a dry place, protected from light, at a temperature of 8° to 25°C. Shelf life: 3 years.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Special Instructions

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

Take levofloxacin at least 2 hours before or 2 hours after taking magnesium/aluminum antacids, or sucralfate, or other drugs containing calcium, iron or zinc.

Due to possible photosensitivity during the treatment period and for 5 days after the end of treatment with levofloxacin, solar and artificial ultraviolet irradiation should be avoided. If phototoxicity develops, treatment with the drug should be discontinued.

If signs of tendonitis and pseudomembranous colitis appear, levofloxacin is immediately discontinued.

It should be borne in mind that patients with a history of brain damage (stroke, severe trauma) may develop seizures.

With glucose-6-phosphate dehydrogenase deficiency, there is a possible risk of hemolytic reactions.

In patients with diabetes mellitus, blood glucose levels should be carefully monitored during treatment with levofloxacin.

When levofloxacin and warfarin are used concomitantly, monitoring of prothrombin time, INR or other coagulation parameters, as well as monitoring for signs of bleeding is indicated.

Data on the use of the drug Hyleflox (750 mg) during radical or sparing sinusotomy in patients with chronic odontogenic perforated maxillary sinusitis indicate high clinical effectiveness. Microbiological control of the use of the drug showed that the use of the drug 750 mg 1 time / day for 10 days suppresses a number of aggressive bacteria that can cause infectious complications. The results obtained allow us to recommend the drug Hyleflox (750 mg) for the purpose of preventing inflammatory complications of the operation of sparing sinusotomy with plastic surgery of the oroantral communication.

Impact on the ability to drive vehicles and operate machinery

While taking levofloxacin, the patient's ability to concentrate and the speed of psychomotor reactions may be impaired. In this regard, it is necessary to be careful when driving vehicles and engaging in other potentially hazardous activities.

Hyleflox, instructions for use (Method and dosage)

Take orally, before meals, swallowing whole.

For hospital-acquired pneumonia, Hyleflox is prescribed 750 mg once, course 14 days.

For community-acquired pneumonia, Hyleflox is prescribed 500 mg once, course 14 days.

For acute sinusitis - 750 mg for 5 days.

Urinary tract infections (without complications) - 250 mg per day for 3 days, with complications - up to 10 days at the same dose.

For chronic prostatitis - 500 mg for 28 days.

If renal function is impaired, the dose is adjusted. If you have diabetes, you need to monitor your glucose . While taking the drug, the patient's ability to concentrate is impaired.

Indications for use

Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to levofloxacin:

• community-acquired pneumonia;
• complicated urinary tract infections and pyelonephritis;
• chronic bacterial prostatitis;
• infections of the skin and soft tissues;
• for complex treatment of drug-resistant forms of tuberculosis;
• prevention and treatment of anthrax through airborne transmission.

For the treatment of the following infectious and inflammatory diseases, levofloxacin can be used as an alternative to other antimicrobial drugs:

• acute sinusitis;
• exacerbation of chronic bronchitis;
• uncomplicated cystitis.

When using the drug Levofloxacin Ecolevid®, official national recommendations on the proper use of antibacterial drugs, as well as the sensitivity of pathogenic microorganisms in a particular country should be taken into account (see section "Special instructions").

Interaction

The active substance increases the elimination period of cyclosporine and enhances the effect of warfarin .

The effect of levofloxacin is reduced by sucralfate , antacids (aluminum- and magnesium-containing), and iron supplements.

When taken with hypoglycemic drugs there is a risk of developing hyperglycemia and hypoglycemia .

Cimetidine slows down the elimination of levofloxacin .

NSAIDs increase the risk of seizures, and corticosteroids may increase the risk of tendon rupture.

Hyleflox, 5 pcs., 500 mg, film-coated tablets

Hospital-acquired infections caused by Pseudomonas aeruginosa may require combination treatment.

Risk of developing resistance

The prevalence of acquired resistance in cultured strains of microorganisms may vary by geographic region and over time. In this regard, information on drug resistance in a specific country is required. For the treatment of severe infections or if treatment is ineffective, a microbiological diagnosis must be established with the isolation of the pathogen and determination of its sensitivity to levofloxacin.

Methicillin-resistant Staphylococcus aureus

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

Disability and potential irreversible serious adverse reactions associated with fluoroquinolones

The use of fluoroquinolones, including levofloxacin, has been associated with disability and the development of irreversible serious adverse reactions from various body systems that can develop simultaneously in the same patient. Adverse reactions caused by fluoroquinolones include tendonitis, tendon rupture, arthralgia, myalgia, peripheral neuropathy, and nervous system side effects (hallucinations, anxiety, depression, insomnia, headaches, and confusion). These reactions may develop from several hours to several weeks after starting levofloxacin therapy. The development of these adverse reactions was observed in patients of any age or without the presence of previous risk factors. If the first signs or symptoms of any serious adverse reactions occur, use of levofloxacin should be discontinued immediately. Fluoroquinolones, including levofloxacin, should be avoided in patients who have experienced any of these serious adverse reactions.

Patients predisposed to developing seizures

Like other quinolones, levofloxacin should be used with great caution in patients with a predisposition to seizures. Such patients include patients with previous lesions of the central nervous system, such as stroke, severe traumatic brain injury; patients simultaneously taking drugs that lower the seizure threshold of the brain, such as fenbufen and other similar non-steroidal anti-inflammatory drugs, or other drugs that lower the seizure threshold, such as theophylline (see section "Interaction with other drugs").

If seizures develop, treatment with levofloxacin should be discontinued.

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 oral metronidazole) should be started immediately. Drugs that inhibit intestinal motility are contraindicated.

Tendinitis and tendon rupture

Tendinitis has been reported rarely with quinolones, including levofloxacin, and can sometimes lead to rupture of tendons, including the Achilles tendon, and may be bilateral. This side effect may occur within 48 hours of starting treatment or several months after completion of fluoroquinolone therapy. Elderly patients are more prone to developing tendonitis; In patients taking fluoroquinolones, the risk of tendon rupture may be increased with concomitant use of corticosteroids. In addition, post-transplant patients have an increased risk of developing tendonitis, so it is recommended to be careful when prescribing fluoroquinolones to this category of patients. In patients with impaired renal function, the daily dose should be adjusted based on creatinine clearance. Patients should be advised to remain calm at the first sign of tendonitis or tendon rupture and to contact their healthcare provider. If you suspect the development of tendonitis or tendon rupture, you should immediately stop treatment with Hyleflox and begin appropriate treatment of the affected tendon, for example, providing it with sufficient immobilization (see sections “Contraindications” and “Side effects”).

Hypersensitivity reactions

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

Severe bullous reactions

When using levofloxacin, cases of severe bullous skin reactions such as Stevens-Johnson syndrome or toxic epidermal necrolysis have been observed (see section "Side effects"). In case of development of any reactions from the skin or mucous membranes, the patient should immediately consult a doctor and not continue treatment until his consultation.

Disorders of the liver and biliary tract

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

Patients with impaired renal function

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

Preventing the development of photosensitivity reactions

Although photosensitivity develops very rarely with the use of levofloxacin, to prevent its development, patients are not recommended to be unnecessarily exposed to strong solar or artificial ultraviolet irradiation (for example, visiting a solarium) during treatment and for 48 hours after the end of treatment with levofloxacin.

Superinfection

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

QT prolongation

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

When using fluoroquinolones, including levofloxacin, caution should be exercised in patients with known risk factors for prolongation of the QT interval: in patients with uncorrected electrolyte disturbances (with hypokalemia, hypomagnesemia); with congenital long QT syndrome; with heart disease (heart failure, myocardial infarction, bradycardia); while taking medications that can prolong the QT interval, such as class IA and III antiarrhythmic drugs, 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 administration”, “Side effects” and “Overdose”, “Interaction with other drugs”).

Patients with glucose-6-phosphate dehydrogenase deficiency

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

Hypo- and hyperglycemia (dysglycemia)

As with the use of other quinolones, cases of hyperglycemia and hypoglycemia have been observed with the use of levofloxacin. During therapy with levofloxacin, dysglycemia occurred more often in elderly patients and patients with diabetes mellitus receiving concomitant therapy with oral hypoglycemic drugs (for example, glibenclamide) or insulin. When using levofloxacin in such patients, the risk of developing hypoglycemia, including hypoglycemic coma, increases. It is necessary to inform patients about the symptoms of hypoglycemia (confusion, dizziness, ravenous appetite, headache, nervousness, palpitations or increased heart rate, pale skin, perspiration, trembling, weakness). If the patient develops hypoglycemia, treatment with levofloxacin should be stopped immediately and appropriate therapy should be initiated. In these cases, it is recommended to switch to therapy with an antibiotic other than a fluoroquinolone, if possible. When treating with levofloxacin in elderly patients and patients with diabetes mellitus, careful monitoring of blood glucose concentrations is recommended.

Peripheral neuropathy

Sensory and sensorimotor peripheral neuropathy, which may have a rapid onset, has been reported in patients taking fluoroquinolones, including levofloxacin.

If the patient develops symptoms of neuropathy, levofloxacin should be discontinued. This minimizes the possible risk of developing irreversible changes.

Patients should be informed to report any symptoms of neuropathy to their healthcare provider. Fluoroquinolones should not be prescribed to patients with a history of peripheral neuropathy.

Exacerbation of pseudoparalytic myasthenia gravis (myasthenia gravis)

Fluoroquinolones, including levofloxacin, have neuromuscular blocking activity and may increase muscle weakness in patients with myasthenia gravis. Post-marketing adverse reactions, including pulmonary failure requiring mechanical ventilation and death, have been associated with the use of fluoroquinolones in patients with myasthenia gravis.

The use of levofloxacin in a patient with an established diagnosis of pseudoparalytic myasthenia gravis is not recommended (see section "Side effects".

Application for airborne anthrax infection

The use of levofloxacin in humans for this indication is based on susceptibility data from Bacillus anthracis obtained from in vitro and experimental animal studies, as well as limited data from the use of levofloxacin in humans. Treating physicians should refer to national and/or international documents that reflect the collectively developed point of view on the treatment of anthrax.

Psychotic reactions

Psychotic reactions, including suicidal ideation/attempts, have been reported in patients taking fluoroquinolones, including levofloxacin, sometimes after a single dose. In case of development of any side effects from the central nervous system, including mental disorders, treatment with levofloxacin should be stopped immediately and appropriate therapy should be prescribed. In these cases, it is recommended to switch to therapy with an antibiotic other than a fluoroquinolone, if possible. The drug should be prescribed with caution to patients with psychosis or patients with a history of mental illness.

Visual impairment

If any visual impairment develops, immediate consultation with an ophthalmologist is necessary (see section “Side Effects”).

Effect on laboratory tests

In patients taking levofloxacin, the determination of opiates in urine may lead to false-positive results, which should be confirmed by more specific methods. Levofloxacin may inhibit the growth of Mycobacterium tuberculosis and subsequently lead to false-negative results of the bacteriological diagnosis of tuberculosis.

Hyleflox's analogs

Level 4 ATX code matches:
Siflox

Leflobakt

Lefoccin

Gatifloxacin

Ofloxacin

Faktiv

Tigeron

Lebel

Zanotsin

Lomefloxacin

Eleflox

Lomflox

Pefloxacin

Tsiprobay

Sparflo

Tariwid

Zoflox

Abaktal

Moxifloxacin

Levofloxacin

Tavanic , Glevo , Lebel , Levolet , Levostar , Lefokcin , Leflobakt .

Reviews of Hyleflox

In an attempt to expand the spectrum of action of fluoroquinolones are significantly superior to the earlier ones in relation to gram-positive flora , as well as chlamydia , mycobacteria and mycoplasmas Levofloxacin , as an isomer of ofloxacin , combines the high effectiveness of ofloxacin and resistance to biotransformation and belongs to the third generation of fluoroquinolones . It is 2 times more active than ofloxacin and is better tolerated, therefore it is widely used in clinical practice. There are warnings when taking this drug to avoid sun exposure due to the risk of photosensitivity. After normalization of the temperature, Hyleflox tablets are recommended to be taken for another 2-3 days.

Most reviews are positive; effectiveness is noted for bronchitis , sinusitis , and bacterial prostatitis . Side effects include nausea, abdominal pain, joint pain, and stool upset. The occurrence of ventricular arrhythmias is less common with moxifloxacin and levofloxacin .

“... I am very pleased with this medicine. There was severe bronchitis with purulent sputum and fever. Before this I took another antibiotic to no avail. This one helped on the third day.” “...Took it as part of the complex treatment of prostatitis (plus suppositories, injections, prostate massage and laser). I helped, I feel good.” “... Prescribed for bilateral sinusitis for 10 days. It helped well, there were no reactions.” “... After completing a 10-day course of taking this medicine, pain appeared in the knee and elbow joints.” “...When taking the pills, pain in the tendons began, the doctor stopped the drug.” “... It didn’t suit me: I developed severe body aches and severe tremors.” “... I couldn’t withstand 28 days while treating prostatitis. The condition of the gastrointestinal tract has worsened - everything has worsened.”

Hyleflox price, where to buy

You can buy Hyleflox at any pharmacy. The cost of the drug depends on the dose: 5 tablets of 750 mg can be purchased for 817-890 rubles, the same number of tablets of 500 mg for 440-494 rubles.

• Online pharmacies in RussiaRussia

ZdravCity

• Hyleflox tablets p.p.o.
  750 mg 5 pcs. Highglans Laboratories Pvt. Ltd IN RUR 622 order
• Hyleflox tablets p.p.o. 500 mg 5 pcs. Highglans Laboratories Pvt. Ltd IN

  380 rub. order