Levolet R pills 750 mg, 10 pcs.

Composition

Each 750 mg film-coated tablet contains:Active ingredient:levofloxacin hemihydrate 768.7 mg, equivalent to 750 mg of levofloxacin. Auxiliary substances:Microcrystalline cellulose (Avicel PH 101) 76 mg, corn starch 75.3 mg, colloidal silicon dioxide 15 mg, crospovidone 64 mg, hypromellose (15 cps) 21 mg, microcrystalline cellulose (Avicel PH 102) 90 mg, magnesium stearate 15 mg; Film coated:opadray white OY 58900 (hypromellose 5 cP 62.5%, titanium dioxide (E 171) 31.25%, macrogol-400 6.25%) 28 mg

. Pharmacological action

pharmacodynamicafluoroquinolone, a broad-spectrum antimicrobial bactericidal agent. It blocks DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and crosslinking of DNA breaks, suppresses DNA synthesis, and causes deep morphological changes in the cytoplasm, cell wall, and membranes. Levofloxacin is active against the following strains of microorganisms, both in vitro and in vivo. Sensitive microorganisms MPAEROBIC gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus faecalis, Enterococcus spp., Listeria monocytogenes, Staphylococcus coagulase-negative methi-S(J) (methicillin-sensitive/moderately sensitive strains), Staphylococcus aureus methi-S (methicillin-sensitive strains), Staphylococcus epidermidis methi-S (methicillin – sensitive strains), Staphylococcus spp. (CNs-leukotoxin-containing;. Group C and G streptococci (including Streptococcus agalactiae, Streptococcus pneumoniae peni-S / UR (penicillin-sensitive / moderately sensitive/resistant strains)), Streptococcus pyogenes, Viridans streptococci peni-S/R (penicillin-sensitive/ resistant strains). Aerobic gram-negative microorganisms: Acinetobacter baumannil, Acinetobacter spp., Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter spp. (including Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae ampi-S/R (Ampicillin-sensitive/resistant strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxela catarrhalis β+/β – (P-lactamase producing and non-producing strains), Morganella morganii, Neisseria gonorrhoeae non-PPNG/PPNG (penicillinase producing and non-producing strains), Neisseria meningitidis, Pasteurella spp. (including Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (including Pseudomonas aeruginosa), Serratia spp. (including Salmonella spp., Serratia marcescens). anaerobic microorganisms: Bacteroides jragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterum spp., Veilonella 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), Ricketsia spp., Ureaplasma urealyticum. Moderately sensitive microorganisms (MPC>4 mg / l):Aerobic gram-positive microorganisms: Corynebacterium urealiticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis methi-R (methicillin-resistant strains), Staphylococcus haemolyticus methi-R (methicillin-resistant strains). Aerobic gram-negative microorganisms: Burkholderia cepacia, CamPylobacter jejuni, CamPylobacter coli. Anaerobic microorganisms: Bacteroides thetaiotaomicron, Bacteroides vulgatus, Bacteroides ovaius, Prevotella spp., Porphyromonas spp. Resistant microorganisms (MPC>8 mg / l):Aerobic gram-positive microorganisms: Corynebacterium jeikeium, Staphylococcus aureus methi-R (methicillin-resistant strains), Staphylococcus coagulase-negative methi-R (coagulase-negative methicillin-resistant strains). Aerobic gram-negative microorganisms: Alcaligenes xylosoxidans. Other microorganisms: Mycobacterium avium. Pharmacokinetics When taken orally, it is rapidly and almost completely absorbed (food intake has little effect on the speed and completeness of absorption). Bioavailability – 99%. The time to reach the maximum concentration (Tmax) is 1-2 hours; when taking 250 and 500 mg, the average maximum concentration (Cmax) is 2.8 and 5.2 mcg/ml, respectively. Plasma protein binding is 30-40%. It penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, organs of the genitourinary system, polymorphonuclear leukocytes, alveolar macrophages. In the liver, a small portion is oxidized and / or deacetylated. It is excreted mainly by the kidneys through glomerular filtration and tubular secretion. The half-life (half-life) is 6-8 hours. Renal clearance is 70% of the total clearance. Less than 5% of levofloxacin is excreted as metabolites. In the urine, for a period of 24 hours,70% is found unchanged, and for 48 hours – 87% of the dose taken orally. In the feces, for a period of 72 hours,4% of the oral dose is detected. In patients with renal insufficiency, the decrease in drug clearance and its excretion by the kidneys depends on the degree of decrease in creatinine clearance (CC).

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to levofloxacin: – acute bacterial sinusitis; – community-acquired pneumonia; – complicated urinary tract infections (including pyelonephritis); – skin and soft tissue infections (complicated).

Use during pregnancy and lactation

Levofloxacin is contraindicated in pregnant and breast-feeding women.

Contraindications

-Hypersensitivity to levofloxacin, other quinolones or other components of the drug; – impaired renal function (with creatinine clearance less than 20 ml / min due to the inability to dose this dosage form); – epilepsy; – tendon damage with previous treatment with fluoroquinolones; – pseudoparalytic myasthenia gravis;- children and adolescents under 18 years of age (due to incomplete growth of the skeleton, since the risk of damage to cartilage growth points cannot be completely excluded); – pregnancy and lactation. With caution:- in diseases of the central nervous system (CNS), including those suspected of involving the central nervous system, predisposing to seizures and reducing the threshold of convulsive brain activity; – in patients receiving concomitant medications that reduce the threshold of convulsive brain readiness (see the section “Interaction with other drugs”);- in patients with psychoses and psychiatric diseases in the anamnesis;- in patients with latent or manifest glucose-6-phosphate dehydrogenase deficiency (increased risk of hemolytic reactions with quinolones);- in patients with impaired renal function with creatinine clearance of 20-50 ml/min (mandatory monitoring of renal function is required, as well as dosage adjustment, see the section “Dosage and administration”);- in patients with known risk factors for QT prolongation: in elderly patients;- in female patients; in patients with uncorrected electrolyte disorders (with hypokalemia, hypomagnesemia); with congenital QT prolongation syndrome; with heart diseases (heart failure, myocardial infarction, bradycardia); when taking concomitant medications that can prolong the QT interval (see the section “Interaction with other medications”);- in patients with diabetes mellitus receiving oral hypoglycemic drugs (for example, glibenclamide) or insulin (the risk of hypoglycemia increases);- in patients with severe adverse reactions to other fluoroquinolones, such as severe neurological reactions (increased risk of similar adverse reactions with levofloxacin).

Side effects

The following side effects are presented according to the following frequency gradations: very common (≥1/10); common (≥1/100, <1/10); uncommon (≥1/1000, <1/100); rare (≥1/10000, <1/1000); very rare (Data obtained in clinical studies and post-marketing use of the drug: cardiac disturbances are rare: sinus tachycardia, palpitation sensation. Frequency unknown (post-marketing data): prolongation of the QT interval, ventricular arrhythmias, ventricular tachycardia, ventricular tachycardia of the “pirouette” type, which can lead to cardiac arrest (see the sections “Overdose”, “Special instructions”). Disorders of the blood and lymphatic system are often: leukopenia (a decrease in the number of white blood cells in the peripheral blood), eosinophilia (an increase in the number of eosinophils in the peripheral blood). Rarely: neutropenia (decrease in the number of neutrophils in the peripheral blood), thrombocytopenia (decrease in the number of platelets in the peripheral blood). The frequency is unknown (post-marketing data): pancytopenia (decrease in the number of all formed elements in the peripheral blood), agranulocytosis (absence or sharp decrease in the number of granulocytes in the peripheral blood), hemolytic anemia. Nervous system disorders often: headache, dizziness. Infrequently: drowsiness, tremor, dysgeusia (perversion of taste). Rarely: paresthesia, convulsions (see fig.section “Special instructions”). Frequency unknown (post-marketing data): peripheral sensory neuropathy, peripheral sensory-motor neuropathy (see section “Special instructions”), dyskinesia, extrapyramidal disorders, ageusia (loss of taste sensations), parosmia (odour sensation disorder, especially subjective odour sensation, objectively absent), including loss of smell; syncope, benign intracranial hypertension. Visual Impairmentsreferencesexternal links: Visual impairments, such as blurring of the visible image. Frequency unknown (post-marketing data): transient vision loss, uveitis. Hearing disorders and labyrinthine disorders often: vertigo (feeling deflected or whirled, or one’s own body or surrounding objects). Rare: ringing in the ears. Frequency unknown (post-marketing data): hearing loss. Respiratory, thoracic and mediastinal disorders Infrequently: shortness of breath. Frequency unknown (post-marketing data): bronchospasm, allergic pneumonitis. Disorders of the gastrointestinal tract often: diarrhea, vomiting, nausea. Infrequently: abdominal pain, dyspepsia, flatulence, constipation. Frequency unknown (post-marketing data): hemorrhagic diarrhea, which in very rare cases can be a sign of enterocolitis, including pseudomembranous colitis (see section “Special instructions”), pancreatitis. Ventricular and urinary tract disorders frequently: increased serum creatinine. Rare: acute renal failure (for example, due to the development of interstitial nephritis). Disorders of the skin and subcutaneous tissue often: rash, pruritus, urticaria, hyperhidrosis. Frequency unknown (post-marketing data): toxic epidermal necrolysis, Stevens-Johnson syndrome, exudative erythema multiforme, photosensitization reactions (hypersensitivity to sunlight and ultraviolet radiation) (see the section “Special instructions”), leukocytoclastic vasculitis, stomatitis. Reactions from the skin and mucous membranes can sometimes develop even after taking the first dose of the drug. Musculoskeletal system and connective tissue disorders often: arthralgia, myalgia. Rare: tendon involvement, including tendinitis (e. g. Achilles tendon), muscle weakness that can be particularly dangerous in patients with pseudoparalytic myasthenia gravis (see section “Special instructions”). Frequency unknown (post-marketing data): rhabdomyolysis, tendon rupture (for example, Achilles tendon). This side effect may occur within 48 hours after starting treatment and may be bilateral in nature( see also the section “Special instructions”), ligament rupture, muscle rupture, arthritis. Metabolic and nutritional disorders are frequent: anorexia nervosa. Rare: hypoglycemia, especially in patients with diabetes mellitus (possible signs of hypoglycemia: “wolfish” appetite, nervousness, perspiration, trembling). Frequency unknown: hyperglycemia, hypoglycemic coma (see section “Special instructions”). Infectious and parasitic diseases often: fungal infections, development of resistance of pathogenic microorganisms. Vascular disorders rarely: reduced blood pressure. Common disorders often: asthenia. Rare: pyrexia (fever). Frequency unknown: pain (including back, chest, and limb pain). Immune system disorders occasionally: angioedema. Frequency unknown (post-marketing data): anaphylactic shock, anaphylactoid shock. Anaphylactic and anaphylactoid reactions can sometimes develop even after taking the first dose of the drug. Disorders of the liver and biliary tract frequently: increased activity of” liver ” enzymes in the blood (for example, alanine aminotransferase (ALT), aspartate aminotransferase (ACT)), increased activity of alkaline phosphatase (ALP) and gamma-glutamyltransferase (GGT). Infrequently: increased bilirubin concentration in the blood. Frequency unknown (post-marketing data): severe hepatic insufficiency, including cases of acute hepatic insufficiency, sometimes fatal, especially in patients with a severe underlying disease (for example, in patients with sepsis) (see the section “Special instructions”); hepatitis, jaundice. Mental disorders often: insomnia. Infrequently: feeling restless, anxious, confused. Rare: mental disorders (e. g. hallucinations, paranoia), depression, agitation (agitation), sleep disorders, nightmares. Frequency unknown (post-marketing data): mental disorders with self-harm behavioral disorders, including suicidal thoughts and suicide attempts. Other possible adverse effects related to all fluoroquinolones are very rare: attacks of porphyria (a very rare metabolic disease) in patients with porphyria.

Interaction

Levofloxacin increases the T1 / 2 of cyclosporine. The effect of levofloxacin is reduced by drugs that inhibit intestinal motility, sucralfate, magnesium-and aluminum-containing antacids and iron salts (a break between administration of at least 2 hours is necessary). Concomitant use of NSAIDs, theophylline increases convulsive readiness, and corticosteroids increase the risk of tendon rupture. Cimetidine and drugs that block tubular secretion slow down the elimination of levofloxacin. Levofloxacin solution for intravenous administration is compatible with 0.9% sodium chloride solution,5% dextrose solution,2.5% Ringer’s solution with dextrose, combined solutions for parenteral nutrition (amino acids, carbohydrates, electrolytes). Levofloxacin solution for intravenous administration should not be mixed with heparin and solutions that have an alkaline reaction.

How to take, course of administration and dosage

Levolet®preparation R is taken orally once a day. Tablets should be taken without chewing and washed down with a sufficient amount of liquid (from 0.5 to 1 cup). The drug can be taken before meals or at any time between meals. The drug should be taken at least 2 hours before or 2 hours after taking antacids containing magnesium and / or aluminum, iron salts or sucralfate (see the section “Interaction with other drugs”). Doses are determined by the nature and severity of the infection, as well as the sensitivity of the suspected pathogen. Do not exceed the recommended dose. The duration of treatment varies depending on the course of the disease. Considering that the bioavailability of levofloxacin when taken in tablets is 99%, in the case of transferring a patient from an intravenous infusion of Levolet® Application for Levolet ® tablets P continue treatment at the same dose as the intravenous infusion. Recommended dosage regimen and duration of treatment in patients with normal or mildly impaired renal function (creatinine clearance greater than 50 ml / min). Acute bacterial sinusitis: 750 mg 1 time a day, the course of treatment is 5 days. Community-acquired pneumonia caused by Streptococcus pneumoniae (penicillin-sensitive / – moderately sensitive / – resistant), Haemophilus influenzae (ampicillin-sensitive / – resistant), Haemophilus parainfluenzae, Mycoplasma pneumonia, Chlamydia pneumoniae: 750 mg 1 time a day, the course of treatment is 5 days. Complicated urinary tract infections caused by Escherichia coli, Klebsiela pneumoniae, Proteus mirabilis; acute pyelonephritis caused by Escherichia coli, including cases of absent bacteremia: 750 mg 1 time a day, the course of treatment is 5 days. Complicated infections of the skin and soft tissues: 750 mg once a day, the course of treatment is 7-14 days. Dosage regimen in patients with impaired renal function (creatinine clearance 50-20 ml / min). Levofloxacin is mainly excreted through the kidneys, so when treating patients with impaired renal function (creatinine clearance 50 – 20 ml/min), a dose reduction of the drug is required: the recommended dose is 750 mg every 48 hours. Dosage regimen in patients with impaired liver functionin case of impaired liver function, no dosage adjustment is required, since levofloxacin is metabolized in the liver to an extremely small extent. Dosage regimen in elderly patients No dosage adjustment is required for elderly patients, except in cases of reduced creatinine clearance to 50 ml / min or lower.

Special instructions

Hospital infections caused by Pseudomonas aeruginosa (Pseudomonas aeruginosa) may require combined treatment. The prevalence of acquired resistance of the seeded strains of microorganisms may vary depending on the geographical region and over time. Therefore, information on drug resistance in a particular country is required. For the treatment of severe infections or if treatment is ineffective, a microbiological diagnosis should be established with the isolation of the pathogen and determination of its sensitivity to levofloxacin. Methicillin-resistant streptococcus aureus There is a high probability that methicillin-resistant Staphylococcus aureus will be resistant to fluoroquinolones, including levofloxacin. Therefore, levofloxacin is not recommended for the treatment of established or suspected infections caused by methicillin-resistant Staphylococcus aureus, if laboratory tests have not confirmed the sensitivity of this microorganism to levofloxacin. Patients predisposed to seizures Like other quinolones, levofloxacin should be used with great caution in patients with a predisposition to seizures.These patients include patients with previous central nervous system disorders, such as stroke, severe traumatic brain injury; patients receiving concomitant medications that lower the threshold for brain seizure readiness, such as fenbufen and other similar nonsteroidal anti-inflammatory drugs or other drugs that lower the threshold for seizure readiness, such as theophylline (see the section “Interaction with other medications”). Pseudomembranous colitis Diarrhea that develops during or after treatment with levofloxacin, especially severe, persistent and/or bloody, may be a symptom of pseudomembranous colitis caused by Clostridium difficile. If pseudomembranous colitis is suspected, treatment with levofloxacin should be stopped immediately and specific antibiotic therapy (vancomycin, teicoplanin or metronidazole orally) should be initiated immediately. Drugs that inhibit intestinal motility are contraindicated. Tendinitis Rarely observed tendinitis with quinolones, including levofloxacin, can lead to tendon rupture, including the Achilles tendon. This side effect may develop within 48 hours of starting treatment and may be bilateral. Elderly patients are more likely to develop tendinitis. The risk of tendon rupture may increase with concomitant use of corticosteroids. If tendinitis is suspected, treatment with Levolet should be discontinued immediately. P and start appropriate treatment of the affected tendon, for example, by ensuring that it is sufficiently immobilized (see sections “Contraindications” and “Side effects”). Hypersensitivity Reactionsilevofloxacin can cause serious, potentially fatal, hypersensitivity reactions (angioedema, anaphylactic shock), even with the use of initial doses (see the section “Side effects”). Patients should immediately stop taking the drug and consult a doctor. Severe bullous reactionswhen taking levofloxacin, there have been cases of severe bullous skin reactions, such as Stevens-Johnson syndrome or toxic epidermal necrolysis (see the section “Side effects”). In case of any skin or mucosal reactions, the patient should immediately consult a doctor and not continue treatment until after consultation. Liver and biliary tract disorders Cases of hepatic necrosis, including fatal liver failure, have been reported with levofloxacin, mainly in patients with severe underlying medical conditions, such as sepsis (see section “Adverse effects”). Patients should be warned to stop treatment and seek immediate medical attention if signs and symptoms of liver damage appear, such as anorexia, jaundice, dark urine, itching, and abdominal pain. Patients with renal insufficiency Since levofloxacin is mainly excreted through the kidneys, in patients with impaired renal function, mandatory monitoring of renal function is required, as well as dosage adjustment (see the section “Dosage and administration”). When treating elderly patients, it should be borne in mind that patients in this group often have impaired renal function (see the section “Dosage and administration”). Prevention of photosensitization reactions Although photosensitization is very rare when levofloxacin is used, to prevent its development, patients are not recommended to be exposed to strong solar or artificial ultraviolet radiation (for example, to visit a tanning salon) during treatment and within 48 hours after the end of treatment with levofloxacin without special need. SuperinfectioNas with other antibiotics, the use of levofloxacin, especially for a long time, can lead to increased reproduction of microorganisms that are insensitive to it (bacteria and fungi), which can cause changes in the microflora that is normally present in humans. As a result, superinfection may develop. Therefore, it is mandatory to re-evaluate the patient’s condition during treatment, and if superinfection develops during treatment, appropriate measures should be taken. QT prolongation Very rare cases of QT prolongation have been reported in patients taking fluoroquinolones, including levofloxacin. Caution should be exercised when using fluoroquinolones, including levofloxacin, in patients with known risk factors for prolongation of the QT interval: in patients with uncorrected electrolyte disturbances (hypokalemia, hypomagnesemia); with congenital QT prolongation syndrome; with heart diseases (heart failure, myocardial infarction, bradycardia); while taking medications that can prolong the QT interval, such as class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, antipsychotics. Elderly and female patients may be more sensitive to drugs that prolong the QT interval. Therefore, fluoroquinolones, including levofloxacin, should be used with caution (see sections “With caution”, “Dosage and administration”, “Side effects”, “Overdose” and “Interaction with other drugs”). Patients with glucose-6-Phosphate dehydrogenase deficiency Patients with latent or manifest glucose-6-phosphate dehydrogenase deficiency have a predisposition to hemolytic reactions when treated with quinolones, which should be taken into account when treated with levofloxacin. Hypo – and hyperglycemia (dysglycemia)As with other quinolones, hyperglycaemia and hypoglycaemia have been reported with levofloxacin, usually in patients with diabetes mellitus receiving concomitant treatment with oral hypoglycaemic drugs (e. g., glibenclamide) or insulin preparations. Cases of hypoglycemic coma have been reported. Blood glucose monitoring is required in patients with diabetes mellitus (see section “Side effects”). Peripheral neuropathyin patients taking fluoroquinolones, including levofloxacin, sensory and sensorimotor peripheral neuropathy has been reported, the onset of which may be rapid. If the patient develops symptoms of neuropathy, levofloxacin should be discontinued. This minimizes the possible risk of irreversible changes. Exacerbation of pseudoparalytic myasthenia gravisFluoroquinolones, including levofloxacin, are characterized by neuromuscular blocking activity and may increase muscle weakness in patients with pseudoparalytic myasthenia gravis. In the post-marketing period, adverse reactions were observed, including pulmonary insufficiency that required mechanical ventilation, and death, which were associated with the use of fluoroquinolones in patients with pseudoparalytic myasthenia gravis. The use of levofloxacin in patients with an established diagnosis of pseudoparalytic myasthenia gravis is not recommended (see the section “Side effects”). Use in the airborne route of anthrax infectionthe use of levofloxacin in humans for this indication is based on data on the sensitivity of Bacillus anthracis to it, obtained in vitro studies and in experimental studies conducted on animals, as well as on limited data on the use of levofloxacin in humans. Treating physicians should refer to national and / or international documents that reflect a common point of view on the treatment of anthrax. Psychotic reactionswhen using quinolones, including levofloxacin, psychotic reactions have been reported, which in very rare cases progressed to the development of suicidal thoughts and behavioral disorders with self-harm (sometimes after taking a single dose of levofloxacin (see section “Side effects”)). If such reactions develop, treatment with levofloxacin should be discontinued and appropriate therapy should be prescribed. Caution should be exercised when prescribing the drug to patients with psychosis or a history of mental illness. Visual impairment If any visual impairment develops, immediate consultation with an ophthalmologist is necessary (see the section “Side effects”). Effects on laboratory tests in patients taking levofloxacin, the determination of opiates in the urine may lead to false positive results, which should be confirmed by more specific methods. Levofloxacin can inhibit the growth of Mycobacterium tuberculosis and subsequently lead to false negative results of the bacteriological diagnosis of tuberculosis. Side effects of Levolet® P, such as dizziness or vertigo, drowsiness and visual disturbances (see the section “Side effects”), may reduce psychomotor reactions and the ability to concentrate. This can pose a certain risk in situations where these abilities are particularly important (for example, when driving a car, when servicing machines and mechanisms, when performing work in an unstable position).

Form of production

Tablets covered with a film-coated white or almost white color

, capsule-shaped, biconvex.

Storage conditions

At a temperature not exceeding 25%^%C. Keep out of reach of children!

Shelf

life is 3 years.

Active ingredient

Levofloxacin

Conditions of release from pharmacies

By prescription

Dosage form

of the tablet

Purpose

Adults as prescribed by a doctor

Indications

Sinusitis, Pneumonia, Infectious Diseases, Skin Infections, Respiratory Tract Infections, Sinusitis, Boils, Bronchospasm, Urinary Tract Infections

Weight

Weight: 23 g.