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

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.

Hyleflox tablet p/o 750 mg N5 (Heinglass)

Levofloxacin is a synthetic broad-spectrum fluoroquinolone. Inhibits DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA breaks, suppresses DNA synthesis, causes profound morphological changes in the cytoplasm, cell wall and membranes of sensitive microorganisms. Levofloxacin is active against aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (leukotoxin-containing and coagulase-negative methicillin-sensitive/moderately sensitive strains, including methicillin-sensitive strains of Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus spp. (including strains of Staphylococcus groups C and G, Streptococcus agalactiae, Streptococcus pyogenes , penicillin-sensitive/moderately sensitive/resistant strains of Streptococcus pneumoniae, penicillin-sensitive/resistant strains of viridans group Streptococcus); aerobic gram-negative microorganisms: Acinetobacter spp. (including Acinetobacter baumanii), Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter spp. (including Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus spp. (including Haemophilus ducreyi, Haemophilus parainfluenzae, ampicillin-sensitive/resistant strains of Haemophilus influenzae), Helicobacter pylori, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxela catarrhalis (β-lactamase-producing and non-producing strains), Morganella morganii, Neisseria spp. (including Neisseria meningitidis, penicillinase-producing and non-penicillinase-producing strains of Neisseria gonorrhoeae), Pasteurella spp. (including Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida), Proteus spp. (including Proteus mirabilis, Proteus vulgaris), Providencia spp. (including Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (including Pseudomonas aeruginosa), Serratia spp. (including Serratia marcescens), Salmonella spp.; anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterum spp., Veilonella spp.; other microorganisms: Bartonella spp., Chlamydia spp. (including Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis), Legionella pneumophila, Mycobacterium spp. (including Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma spp. (including Mycoplasma hominis, Mycoplasma pneumoniae), Rickettsia spp., Ureaplasma urealyticum. Aerobic gram-positive microorganisms are resistant to the drug: Corynebacterium jeikeium, Staphylococcus spp. (coagulase-negative methicillin-resistant strains, including methicillin-resistant strains of Staphylococcus aureus); aerobic gram-negative microorganisms: Alcaligenes xylosoxidans; other microorganisms: Mycobacterium avium.

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.

Hyleflox film-coated tablets 750 mg 5 pcs. in Moscow

Pharmacological action: Pharmacodynamics

Has a wide spectrum of action. Inhibits bacterial topoisomerase IV and DNA gyrase (type II topoisomerases) - enzymes necessary for replication, transcription, repair and recombination of bacterial DNA. In concentrations equivalent to or slightly higher than inhibitory concentrations, it most often has a bactericidal effect. In vitro

Resistance to levofloxacin, resulting from spontaneous mutations, is rare (10−9−10−10). Although cross-resistance has been observed between levofloxacin and other fluoroquinolones, some organisms resistant to other fluoroquinolones may be sensitive to levofloxacin.

Installed in vitro

and confirmed in clinical studies to be effective against gram-positive bacteria -
Enterococcus faecalis, Staphylococcus aureus
(methicillin-sensitive strains),
Staphylococcus epidermidis
(methicillin-sensitive strains)
, Staphylococcus saprophyticus, Streptococcus pneumoniae
(including multi-resistant strains -
MDRSP
*),
Streptococcus pyogenes
;
gram-negative bacteria - Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Legionella pneumophila, Moraxella catarrhalis, Proteus mirabilis, Pseudomonas aeruginosa,
Serratia
marcescens
and other microorganisms -
Chlamydia pneumoniae, Mycoplasma pneumoniae.
Against most (≥90%) strains of the following microorganisms in vitro

The MIC of levofloxacin has been established (2 μg/ml or less), however, the effectiveness and safety of the clinical use of levofloxacin in the treatment of infections caused by these pathogens has not been established in adequate and well-controlled studies: gram-positive bacteria -
Staphylococcus haemolyticus, Streptococcus
(group C/F),
Streptococcus
(group G),
Streptococcus agalactiae, Streptococcus milleri
,
Streptococcus viridans
,
Bacillus anthracis
;
gram-negative bacteria - Acinetobacter lwoffii, Acinetobacter baumannii, Bordetella pertussis, Citrobacter (diversus) koseri, Citrobacter freundii, Enterobacter aerogenes, Enterobacter sakazakii, Klebsiella oxytoca, Morganella morganii, Pantoea (Enterobacter) agglomerans, Proteus vulgaris, Providencia rettgeri, Providencia s tuartii, Pseudomonas fluorescens
,
Yersinia pestis
;
gram-positive anaerobes - Clostridium perfringens.
May be effective against microorganisms resistant to aminoglycosides, macrolides and beta-lactam antibiotics (including penicillin).

* Strains with multiple resistance to antibiotics ( Multi-drug resistant Streptococcus pneumoniae

-
MDRSP
) include strains resistant to two or more of the following antibiotics: penicillin (with MIC ≥2 μg/ml), second generation cephalosporins (for example, cefuroxime), macrolides, tetracyclines and trimethoprim/sulfamethoxazole.

Clinical researches

Efficacy of levofloxacin in the treatment of community-acquired bacterial pneumonia (7-14 day dosing regimen)

studied in two prospective multicenter clinical studies.
The first randomized study, which included 590 patients with community-acquired bacterial pneumonia, compared the effectiveness of levofloxacin at a dose of 500 mg once daily orally or intravenously for 7–14 days and cephalosporins with a total treatment duration of 7–14 days; if the presence of an atypical pneumonia pathogen was suspected or confirmed, patients in the comparison group could additionally receive erythromycin or doxycycline. The clinical effect (cure or improvement) on days 5–7 after completion of levofloxacin therapy was 95% compared to 83% in the comparison group. In the second study, which included 264 patients who received levofloxacin 500 mg once daily orally or intravenously for 7–14 days, the clinical response was 93%. In both studies, the effectiveness of levofloxacin in the treatment of atypical pneumonia caused by Chlamydia pneumoniae, Mycoplasma pneumoniae
and
Legionella pneumoniae
was 96, 96 and 70%, respectively.
The degree of microbiological eradication in both studies was depending on the pathogen: H.influenzae
- 98%,
S.pneumoniae
- 95%,
S.aureus
- 88%,
M.catarrhalis
- 94%,
H.parainfluenzae
- 95%,
K.pneumoniae
- 100%.

Levofloxacin is effective for the treatment of community-acquired pneumonia caused by strains of Streptococcus pneumoniae

multidrug resistant
(MDRSP).
After microbiological evaluation
of MDRSP
isolates isolated from 40 patients, it was found that 38 patients (95%) achieved clinical (recovery or improvement) and bacteriological effect after completion of levofloxacin therapy. The degree of bacteriological eradication was for different pathogens: penicillin-resistant strains - 94.1%, strains resistant to 2nd generation cephalosporins - 96.9%, strains resistant to macrolides - 96.6%, strains resistant to trimethoprim/sulfamethoxazole - 89.5%, strains resistant to tetracyclines - 100%.

Efficacy and safety of levofloxacin in community-acquired bacterial pneumonia (5-day dosing regimen)

were evaluated in a double-blind, randomized, prospective, multicenter study in 528 outpatient and hospitalized adult patients with clinically and radiologically defined mild to severe community-acquired pneumonia, comparing levofloxacin 750 mg (IV or orally every day for five days) or at a dose of 500 mg (iv or orally daily for 10 days).
The clinical effect (improvement or recovery) was 90.9% in the group receiving levofloxacin 750 mg and 91.1% in the group receiving levofloxacin 500 mg. Microbiological effectiveness (degree of bacteriological eradication) of a 5-day dosing regimen depending on the pathogen: S. pneumoniae
- 95%,
Haemophilus influenzae
- 100%,
Haemophilus pararainfluenzae
- 100%,
Mycoplasma pneumoniae
- 96%,
Chlamydophila pneumoniae
- 87%.

Efficacy and safety of levofloxacin in the treatment of acute bacterial sinusitis

(5- and 10-14-day dosing regimens) caused by
Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis,
was evaluated in a double-blind, randomized, prospective, multicenter study in 780 outpatients who received levofloxacin 750 mg orally once daily. for 5 days or 500 mg for 10 days. The clinical effect of levofloxacin (complete or partial resolution of symptoms of acute bacterial sinusitis to the extent that further antibiotic therapy was not considered necessary) according to microbiological assessment was 91.4% in the group receiving levofloxacin 750 mg and 88.6% in the group receiving levofloxacin 750 mg and group receiving 500 mg levofloxacin.

Efficacy of levofloxacin in the treatment of complicated urinary tract infections and acute pyelonephritis (5-day dosing regimen)

was evaluated in 1109 patients in a randomized, double-blind, multicenter clinical trial in which patients received levofloxacin 750 mg IV or orally once daily for 5 days (546 patients) or ciprofloxacin 400 mg IV or 500 mg orally twice daily for 10 days (563 patients).
The effectiveness of levofloxacin was assessed after 10–14 days by the degree of bacteriological eradication and was, depending on the pathogen: Escherichia coli
- 90%,
Klebsiella pneumoniae
- 87%,
Proteus mirabilis
- 100%.

Efficacy and safety of levofloxacin in the treatment of complicated urinary tract infections and acute pyelonephritis (10-day dosing regimen)

evaluated a 10-day course of treatment with levofloxacin 250 mg orally once daily in 285 patients with uncomplicated urinary tract infections, complicated urinary tract infections (mild to moderate), and acute pyelonephritis (mild to moderate) in a randomized, double-blind, multicenter clinical trial. Microbiological effectiveness, measured by bacteriological eradication of microorganisms, was approximately 93%.

Efficacy of levofloxacin for infectious lesions of the skin and skin structures

studied in an open, randomized comparative study that included 399 patients who received levofloxacin at a dose of 750 mg/day (iv, then orally) or a comparison drug for (10±4.7) days. Surgical procedures for complicated infections (excision of dead tissue and drainage) shortly before the start or during antibacterial therapy (as part of complex therapy) were performed in 45% of patients receiving levofloxacin and 44% of patients in the comparison group. Among patients who were observed for 2–5 days after the end of drug therapy, the clinical effect was 116/138 (84.1%) in the group receiving levofloxacin and 106/132 (80.3%) in the comparison group.

The effectiveness of levofloxacin was also demonstrated in a multicenter randomized open trial in the treatment of nosocomial pneumonia

and in a multicenter, randomized, double-blind study in the treatment
of chronic bacterial prostatitis.
Eye drops

The clinical effect of levofloxacin 0.5% eye drops in randomized, double-blind, multicenter controlled trials in the treatment of bacterial conjunctivitis was 79% at the end of treatment (days 6–10). The degree of microbiological eradication reached 90%.

Pharmacokinetics

Absorption.

After oral administration, it is quickly and completely absorbed from the gastrointestinal tract; the absolute bioavailability of 500 mg and 750 mg tablets of levofloxacin is 99%. Cmax is reached within 1–2 hours. When taken simultaneously with food, the time to reach Cmax slightly increases (by 1 hour) and Cmax decreases slightly (by 14%), thus, levofloxacin can be prescribed regardless of food intake. After a single intravenous administration to healthy volunteers at a dose of 500 mg (infusion over 60 minutes), Cmax was (6.2 ± 1) μg/ml, at a dose of 750 mg (infusion over 90 minutes) - (11.5 ± 4 ) µg/ml. The pharmacokinetics of levofloxacin is linear and predictable with single and repeated oral and intravenous administration. Constant concentration in plasma is achieved after 48 hours when taking 500–750 mg 1 time per day. With repeated administration to healthy volunteers, the Cmax values ​​were: for oral administration 500 mg/day - (5.7 ± 1.4) μg/ml, 750 mg/day - (8.6 ± 1.9) μg/ml; with intravenous administration, 500 mg/day - (6.4±0.8) µg/ml, 750 mg/day - (12.1±4.1) µg/ml. The plasma concentration profile of levofloxacin after intravenous administration is similar to that after oral administration at an equivalent dose.

Distribution.

The average Vd is 74–112 L after single and repeated doses of 500 and 750 mg.
Widely distributed in body tissues, penetrates well into lung tissue (concentration in the lungs is 2–5 times higher than the concentration in plasma). In vitro
, in the concentration range corresponding to clinical values ​​(1–10 μg/ml), binding to plasma proteins (mainly albumin) is 24–38% and does not depend on the concentration of levofloxacin.

Metabolism and excretion.

Stereochemically stable in plasma and urine, does not convert to its enantiomer, D-ofloxacin. It is practically not metabolized in the body. It is excreted predominantly unchanged in the urine (about 87% of the dose within 48 hours), small amounts in feces (less than 4% within 72 hours). Less than 5% is determined in urine in the form of metabolites (desmethyl, nitric oxide), which have little specific pharmacological activity.

Terminal T1/2 from plasma is 6–8 hours after a single or repeated administration orally or intravenously. Total Cl is 144–226 ml/min, renal Cl is 96–142 ml/min, excretion is carried out by glomerular filtration and tubular secretion. Concomitant use of cimetidine or probenecid leads to a decrease in renal Cl by 24 and 35%, respectively, indicating secretion of levofloxacin by the proximal tubules. Levofloxacin crystals were not detected in freshly collected urine.

Special patient groups

Age, gender, race.

The pharmacokinetics of levofloxacin does not depend on the age, gender and race of patients.

After administration of 500 mg orally to healthy male volunteers, T1/2 averaged 7.5 hours compared to 6.1 hours in women; the differences were associated with the characteristics of renal function in men and women and were not of clinical significance.

Features of pharmacokinetics depending on race were studied by covariance analysis of data from 72 subjects: 48 representatives of the Caucasian race and 24 others; no differences were found in terms of total clearance and volume of distribution.

Elderly age.

The pharmacokinetics of levofloxacin in elderly patients does not differ significantly when individual differences in creatinine clearance values ​​are taken into account. After a single oral dose of 500 mg levofloxacin, T1/2 in healthy elderly patients (66–80 years) was 7.6 hours compared to 6 hours in younger patients; the differences are explained by variability in renal function and are not clinically significant. No dose adjustment is required in elderly patients.

Kidney failure.

In patients with impaired renal function (Cl creatinine <50 ml/min), the clearance of levofloxacin is significantly reduced and T1/2 is increased; dose adjustment is required to prevent accumulation. Hemodialysis and long-term ambulatory peritoneal dialysis do not remove levofloxacin from the body and therefore do not require additional doses.

Liver failure.

Pharmacokinetic studies have not been conducted in patients with liver disease. Since the metabolism of levofloxacin is negligible, liver damage is not expected to influence pharmacokinetics.

Children

. After a single intravenous administration of levofloxacin at a dose of 7 mg/kg in children aged 6 months to 16 years, the drug was eliminated faster than in adult patients. Subsequent pharmacokinetic analysis shows that a dosing regimen of 8 mg/kg (not more than 250 mg per dose) every 12 hours in children 6 months - 17 years at steady state will achieve plasma AUC0-24 and Cmax values ​​comparable to those in adults patients at a dose of levofloxacin 500 mg every 24 hours.

Pharmacokinetics of levofloxacin in patients with severe community-acquired pneumonia

does not differ from that in healthy volunteers.

Study of the pharmacokinetics of levofloxacin when used as 0.5% eye drops

was carried out on 15 healthy adult volunteers. Levofloxacin plasma concentrations were measured at various time points throughout the 15-day course of use. The average plasma concentration of levofloxacin 1 hour after instillation varied from 0.86 ng/ml on the first day to 2.05 ng/ml on the fifteenth day. Cmax of levofloxacin in plasma was 2.25 ng/ml and was achieved on the 4th day after 2 days of use every 2 hours (up to 8 times a day). The Cmax of levofloxacin achieved on day 15 was more than 1000 times lower than the concentration observed after oral administration of standard doses of levofloxacin.

In studies in healthy adult volunteers (n=30), the mean tear film concentrations of levofloxacin measured 4 and 6 hours after instillation were 17.0 mcg/mL and 6.6 mcg/mL, respectively (clinical significance unknown) .

Experimental toxicology and/or pharmacology

Levofloxacin and other fluoroquinolones have been shown to cause arthropathy in young growing animals of most species tested.

Oral administration of levofloxacin at a dose of 40 mg/kg/day in 3-month-old dogs resulted in clinically significant arthropathy and discontinuation of dosing on day 8 of the planned 14 days. Minor musculoskeletal clinical effects in the absence of gross pathological or histopathological abnormalities were observed with the lowest dose level of 2.5 mg/kg/day (approximately 0.2 times the pediatric dose based on AUC comparisons). Synovitis and articular cartilage lesions were observed at doses of 10 and 40 mg/kg (approximately 0.7 and 2.4 times the pediatric dose based on AUC comparisons). Gross articular cartilage pathology and histopathological changes persisted until the end of the 18-week recovery period in dogs treated with levofloxacin 10 and 40 mg/kg/day.

In animal experiments, administration of levofloxacin orally or intravenously to immature rats and dogs resulted in an increase in the incidence of osteochondrosis. Histopathological examination of weight-bearing joints in immature dogs exposed to levofloxacin revealed persistent cartilage lesions. Other fluoroquinolones also cause similar erosive changes in weight-bearing joints and other manifestations of arthropathy in immature animals of various species.

In immature dogs (4–5 months of age), oral administration at a dose of 10 mg/kg/day for 7 days or IV at a dose of 4 mg/kg/day for 14 days led to the development of arthropathy. Oral administration of 300 mg/kg/day for 7 days or intravenous administration of 60 mg/kg/day for 4 weeks caused arthropathy in immature rats.

In studies in mice, levofloxacin had phototoxic effects similar in severity to ofloxacin, but less pronounced compared to other fluoroquinolones.

Although crystalluria was observed in rats given IV in some studies, urinary crystals did not form in the bladder, were detected only after urination, and were not associated with nephrotoxicity.

In experiments on mice, the stimulating effect of fluoroquinolones on the central nervous system was enhanced when used simultaneously with NSAIDs.

When administered rapidly intravenously to dogs at a dose of 6 mg/kg or more, levofloxacin caused a hypotensive effect, presumably due to the release of histamine.

in vitro studies

and
in vivo
, levofloxacin within therapeutic concentrations did not have an inducing or inhibitory effect on enzyme systems, i.e., an enzyme-mediated effect on the metabolism of other drugs is not expected.

Carcinogenicity, mutagenicity, effect on fertility

In intravital biological studies in rats, levofloxacin did not exhibit carcinogenic properties when administered daily orally for 2 years at doses up to 100 mg/kg/day (1.4 times the MRDC (750 mg), based on body surface area). Levofloxacin, at any dosage regimen, did not reduce the time to development of UV-induced skin tumors in hairless albino mice (Skh-1) and thus did not exhibit photocarcinogenic properties under experimental conditions. The concentration of levofloxacin in the skin tissues of hairless mice was in the range of 25–42 μg/g when using the maximum dose in the photocarcinogenicity study (300 mg/kg/day). For comparison, in humans, the concentration of levofloxacin in skin tissues when administered at a dose of 750 mg averages 11.8 mcg/g with Cmax in plasma.

Did not show mutagenic properties in the following studies: Ames test on S. Typhimurium

and
E.Coli,
hypoxanthine-guanine phosphoribosyltransferase test in Chinese hamster ovary cells, micronucleus test in mice, dominant lethal mutation test in mice, unscheduled DNA synthesis test in rats, sister chromatid exchange test in mice.
in vitro
tests for chromosomal aberrations (on the CHL cell line) and sister chromatid exchange (on the CHL/IU cell line).

It had no effect on the fertility and reproductive function of rats when administered orally at a dose of 360 mg/kg/day (4.2 times the MRDC, based on body surface area) or intravenously at a dose of 100 mg/kg/day (in 1.2 times the MRFC, in terms of body surface area).

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

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 750 mg 5 pcs. film-coated tablets

pharmachologic effect

Levofloxacin is a synthetic broad-spectrum fluoroquinolone.
Inhibits DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA breaks, suppresses DNA synthesis, causes profound morphological changes in the cytoplasm, cell wall and membranes of sensitive microorganisms. Levofloxacin is active against aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (leukotoxin-containing and coagulase-negative methicillin-sensitive/moderately sensitive strains, including methicillin-sensitive strains of Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus spp. (including strains of Staphylococcus groups C and G, Streptococcus agalactiae, Streptococcus pyogenes , penicillin-sensitive/moderately sensitive/resistant strains of Streptococcus pneumoniae, penicillin-sensitive/resistant strains of viridans group Streptococcus); aerobic gram-negative microorganisms: Acinetobacter spp. (including Acinetobacter baumanii), Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter spp. (including Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus spp. (including Haemophilus ducreyi, Haemophilus parainfluenzae, ampicillin-sensitive/resistant strains of Haemophilus influenzae), Helicobacter pylori, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxela catarrhalis (beta-lactamase producing and non-producing strains), Morganella morganii, Neisseria spp. (including Neisseria meningitidis, penicillinase-producing and non-penicillinase-producing strains of Neisseria gonorrhoeae), Pasteurella spp. (including Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida), Proteus spp. (including Proteus mirabilis, Proteus vulgaris), Providencia spp. (including Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (including Pseudomonas aeruginosa), Serratia spp. (including Serratia marcescens), Salmonella spp.; anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterum spp., Veilonella spp.; other microorganisms: Bartonella spp., Chlamydia spp. (including Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis), Legionella pneumophila, Mycobacterium spp. (including Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma spp. (including Mycoplasma hominis, Mycoplasma pneumoniae), Rickettsia spp., Ureaplasma urealyticum.

Aerobic gram-positive microorganisms are resistant to the drug: Corynebacterium jeikeium, Staphylococcus spp. (coagulase-negative methicillin-resistant strains, including methicillin-resistant strains of Staphylococcus aureus); aerobic gram-negative microorganisms: Alcaligenes xylosoxidans; other microorganisms: Mycobacterium avium.

Composition and release form Hyleflox 750 mg 5 pcs. film-coated tablets

Tablets - 1 tablet:

• Active substance: levofloxacin (in the form of hemihydrate) 750 mg.
• Excipients: 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.

Description of the dosage form

Light orange to orange film-coated tablets, oval, biconvex, scored on one side; at the break - the core is from white with a yellow tint to yellow.

Directions for use and doses

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

For adult patients with normal renal function (creatinine clearance > 50 ml/min), use in accordance with the regimens 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 (CR

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

Pharmacokinetics

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 µg/ml, 5.2 µg/ml and 8 µg/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 Hyleflox 750 mg 5 pcs. film-coated tablets

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).

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.

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

Application of Hyleflox 750 mg 5 pcs. film-coated tablets during pregnancy and breastfeeding

The drug is contraindicated during pregnancy and lactation.

Use in children

Contraindicated in children and adolescents under 18 years of age.

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.

Overdose

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

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

Side effects Hyleflox 750 mg 5 pcs. film-coated tablets

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.

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

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

Drug interactions

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.

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

  RUR 368 order

Hyleflox

Levofloxacin is a synthetic broad-spectrum fluoroquinolone. Inhibits DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA breaks, suppresses DNA synthesis, causes profound morphological changes in the cytoplasm, cell wall and membranes of sensitive microorganisms.

Levofloxacin is active against aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (leukotoxin-containing and coagulase-negative methicillin-sensitive/moderately sensitive strains, including methicillin-sensitive strains of Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus spp. (including strains of Staphylococcus groups C and G, Streptococcus agalactiae, Streptococcus pyogenes , penicillin-sensitive/moderately sensitive/resistant strains of Streptococcus pneumoniae, penicillin-sensitive/resistant strains of viridans group Streptococcus); aerobic gram-negative microorganisms: Acinetobacter spp. (including Acinetobacter baumanii), Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter spp. (including Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus spp. (including Haemophilus ducreyi, Haemophilus parainfluenzae, ampicillin-sensitive/resistant strains of Haemophilus influenzae), Helicobacter pylori, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxela catarrhalis (beta-lactamase producing and non-producing strains), Morganella morganii, Neisseria spp. (including Neisseria meningitidis, penicillinase-producing and non-penicillinase-producing strains of Neisseria gonorrhoeae), Pasteurella spp. (including Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida), Proteus spp. (including Proteus mirabilis, Proteus vulgaris), Providencia spp. (including Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (including Pseudomonas aeruginosa), Serratia spp. (including Serratia marcescens), Salmonella spp.; anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterum spp., Veilonella spp.; other microorganisms: Bartonella spp., Chlamydia spp. (including Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis), Legionella pneumophila, Mycobacterium spp. (including Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma spp. (including Mycoplasma hominis, Mycoplasma pneumoniae), Rickettsia spp., Ureaplasma urealyticum.

Aerobic gram-positive microorganisms are resistant to the drug: Corynebacterium jeikeium, Staphylococcus spp. (coagulase-negative methicillin-resistant strains, including methicillin-resistant strains of Staphylococcus aureus); aerobic gram-negative microorganisms: Alcaligenes xylosoxidans; other microorganisms: Mycobacterium avium.

Pharmacokinetics

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.