Leflobact
Leflobact: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Leflobact
ATX code: J01MA12
Active ingredient: levofloxacin (levofloxacin)
Producer: Sintez, JSC (Russia)
Description and photo updated: 22.11.2018
Prices in pharmacies: from 139 rubles.
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Leflobact is an antibacterial drug, fluoroquinolone.
Release form and composition
Leflobact dosage forms:
- film-coated tablets: yellow, at a dosage of 250 mg - round, biconvex, at a dosage of 500 mg - oval (tablets 250 mg: in blisters of 5 pcs., in a cardboard box 1 or 2 packs; in blisters 7 or 10 pcs., in a cardboard box 1 package; in a polymer can 7 or 10 pcs., in a cardboard box 1 can; tablets 500 mg: in blisters of 5 pcs., in a cardboard box 1 or 2 packages; in contour cell packs of 7 pcs., in a cardboard box 1 package; in a polymer can 7 or 10 pcs., in a cardboard box 1 can);
- solution for infusion 0.5%: clear liquid, greenish-yellow color (100 ml in an orange glass bottle or in a glass bottle, in a cardboard box 1 bottle or bottle).
1 tablet contains:
- active substance: levofloxacin (in the form of hemihydrate) - 250 mg or 500 mg;
- auxiliary components: lactose, calcium stearate, povidone, starch 1500, crospovidone (Kollidon CL-M), potato starch, microcrystalline cellulose, talc;
- shell composition: titanium dioxide, hypromellose, tropeolin 0 (resorcinol yellow), macrogol.
1 ml of solution contains:
- active substance: levofloxacin (in the form of hemihydrate) - 5 mg;
- auxiliary components: sodium chloride, water for injection.
Pharmacological properties
Pharmacodynamics
Leflobact is an antimicrobial bactericidal synthetic drug from the group of fluoroquinolones. Its active ingredient - levofloxacin, being the levorotatory isomer of ofloxacin, has a wide spectrum of antibacterial activity, which covers various streptococci, including pneumococci. The mechanism of action of the drug is due to the ability of levofloxacin to block DNA (deoxyribonucleic acid) -gyrase (topoisomerase II) and topoisomerase IV of bacteria, disrupt the process of supercoiling and stitching of DNA breaks, inhibit DNA synthesis. Causing deep morphological changes in the cell wall, membrane and cytoplasm of microorganisms, the action of levofloxacin does not apply to the enzymes of the cells of the human body.
At MIC (minimum inhibitory concentration) less than 2 mg / ml, the following microorganisms are susceptible to levofloxacin in vitro and in vivo:
- aerobic gram-positive: Corynebacterium diphtheriae, Staphylococcus speciales (spp.) coagulase-negative (strains moderately sensitive and sensitive to methicillin), methicillin-sensitive strains Staphylococcus aureus and Staphylococcus epidermidis agalis, Streptococcus epidermidis, Streptococcus spp. (group C and G), sensitive, moderately sensitive and resistant to penicillin strains of Streptococcus pneumoniae, sensitive and resistant to penicillin strains of Streptococcus viridans, Enterococcus spp. (except Enterococcus faecium), Enterococcus faecalis, Listeria monocytogenes;
- aerobic gram-negative: Acinetobacter spp. (including Acinetobacter calcoaceticus, Acinetobacter baumannii), Bordetella pertussis, Actinobacillus actinomycetemcomitans, Eikenella corrodens, Citrobacter freundii, Citrobacter diversus, Escherichia coli, Enterobacter spp. (including Enterobacter aerogenes, Enterobacter cloacae, Enterobacter agglomerans), Gardnerella vaginalis, Helicobacter pylori, Haemophilus ducreyi, Haemophilus parainfluenzae, ampicillin sensitive and resistant strains of Haemophilus influenzae, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella catarrhalis (non-beta-lactamase-producing and non-beta-lactamase-producing strains), Neisseria meningitidis, Neisseria gonorrhoeae, Morganella morganii, Pasteurella spp. (including Pasteurella canis, Pasteurella multocida, Pasteurella dagmatis), Proteus vulgaris,Proteus mirabilis, Pseudomonas spp., Pseudomonas aeruginosa, Providencia spp. (including Providencia stuartii, Providencia rettgeri), Salmonella spp., Serratia marcescens and other Serratia spp.;
- anaerobic: Bifidobacterium spp., Bacteroides fragilis, Peptostreptococcus spp., Clostridium perfringens, Fusobacterium spp., Veillonella spp., Propionibacterium spp.;
- others: Chlamydia psittaci, Chlamydia (Chlamydophila) pneumoniae, Chlamydia trachomatis, Bartonella spp., Mycobacterium spp. (including Mycobacterium tuberculosis, Mycobacterium leprae), Legionella spp. (including Legionella pneumophila), Mycoplasma hominis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Rickettsia spp.
Moderate sensitivity (with a MIC of 4 mg / ml and higher) to levofloxacin is shown by the following microorganisms:
- aerobic gram-positive: Corynebacterium xerosis, Corynebacterium urealyticum, Enterococcus faecium, methicillin-resistant strains of Staphylococcus epidermidis and Staphylococcus haemolyticus;
- aerobic gram-negative: Burkholderia cepacia, Campylobacter coli, Campylobacter jejuni;
- anaerobic: Bacteroides vulgatus, Bacteroides thetaiotaomicron, Bacteroides ovatus, Porphyromonas spp., Prevotella spp.
Resistance to levofloxacin (with a MIC of 8 mg / ml and higher) is shown by the following microbes:
- aerobic gram-positive: methicillin-resistant strains of Staphylococcus aureus, Corynebacterium jeikeium, coagulase-negative methicillin-resistant strains of Staphylococcus spp.;
- aerobic gram-negative: Alcaligenes xylosoxidans;
- others: Mycobacterium avium.
Pharmacokinetics
With single or multiple oral administration and intravenous (iv) administration of Leflobact, the linear character and predictability of the pharmacokinetics of levofloxacin are preserved.
Its concentration in blood plasma is similar when using the same doses of solution and tablets.
After oral administration, the absorption of the drug occurs in the gastrointestinal tract quickly and practically in full, while the simultaneous intake of food practically does not affect the completeness and rate of absorption. The bioavailability of levofloxacin is 99%, its maximum concentration (Cmax) is reached after 1-2 hours. After oral administration of 250 mg of the drug, it is 0.0028 mg / ml, 500 mg - 0.0052 mg / ml. The volume of distribution (Vd) averages 89–112 liters after intravenous administration at a dose of 500 mg once and repeatedly. Cmax after a single intravenous injection of 500 mg of the drug reaches approximately 0.0062 mg / ml for 1 hour.
Plasma protein binding - 30-40%.
The good penetrating ability of the active substance allows it to easily pass into sputum, bronchial mucosa, prostate gland and other organs of the genitourinary system, cerebrospinal fluid, bone tissue, polymorphonuclear leukocytes, alveolar macrophages. The level of concentration of levofloxacin in the lungs exceeds its plasma values.
A small portion is metabolized in the liver by oxidation and / or deacetylation.
Through the kidneys, by glomerular filtration and tubular secretion, most of the levofloxacin is excreted unchanged and less than 5% - in the form of metabolites.
Within 72 hours after oral administration, 4% of the substance is found in the feces.
T 1/2 (half-life) when taking Leflobact tablets is 6-8 hours, with intravenous administration - 5.7-7.1 hours.
Renal clearance is 70% of the total clearance. In renal failure, the clearance of the drug and its excretion through the kidneys depend on the degree of decrease in creatinine clearance (CC).
Indications for use
The use of all forms of Leflobact's release is indicated for the treatment of the following infectious and inflammatory diseases caused by bacteria sensitive to levofloxacin:
- community-acquired pneumonia;
- acute pyelonephritis, urogenital chlamydia, prostatitis;
- suppurating atheromas, boils, abscess.
In addition, Leflobact solution for infusion is prescribed for such diseases:
- chronic bacterial prostatitis;
- intra-abdominal infections;
- septicemia or bacteremia associated with the above bacterial pathologies.
Additional indications for taking Leflobact in tablet form:
- Chronical bronchitis;
- otitis media, sinusitis;
- drug-resistant forms of tuberculosis - as part of complex therapy.
Contraindications
- damage to the tendons against the background of previous treatment with quinolones;
- epilepsy;
- period of pregnancy;
- breast-feeding;
- age up to 18 years;
- hypersensitivity to drugs of the quinolone group;
- individual intolerance to the components of Leflobact.
In addition, taking pills is contraindicated in patients with impaired renal function (CC less than 20 ml / min) and during hemodialysis.
According to the instructions, Leflobact is recommended to be prescribed with caution for the treatment of patients with glucose-6-phosphate dehydrogenase deficiency and in old age.
The solution should be used with caution in diabetes mellitus, pseudoparalytic myasthenia gravis, renal failure, hepatic porphyria, organic diseases of the central nervous system (CNS), psychosis and other mental disorders in history, brain damage in history (severe trauma, stroke), predisposition to convulsive reactions (a history of cerebrovascular accidents, atherosclerosis of cerebral vessels), hypokalemia, hypomagnesemia and other electrolyte imbalances, bradycardia, heart failure, myocardial infarction, congenital lengthening of the QT interval, in patients with risk factors for prolongation of the QT interval, the use of fenbufen, theophylline (drugs that lower the threshold of convulsive readiness of the brain),in combination with drugs causing prolongation of the QT interval (macrolides, antiarrhythmics of classes IA and III, tricyclic antidepressants, antipsychotics, tetracyclic antidepressants, imidazole derivatives, antifungal and antihistamines, including astemizole, terfenadine, ebastine).
Instructions for the use of Leflobact: method and dosage
Film-coated tablets
Leflobact tablets should be taken orally, swallowed whole and washed down with a sufficient amount (100-200 ml) of liquid, between meals or before meals.
Recommended dosage according to indications:
- community-acquired pneumonia: 500 mg 1–2 times a day, the duration of the course of therapy is 7–14 days;
- sinusitis: 500 mg once a day, the duration of the course of therapy is 10-14 days;
- exacerbation of chronic bronchitis: 250–500 mg once a day, the duration of the course of therapy is 7–10 days;
- uncomplicated urinary tract infections: 250 mg once a day, the duration of the course of therapy is 3 days;
- pyelonephritis and other complicated urinary tract infections: 250 mg once a day, the duration of the course of therapy is 7-10 days;
- prostatitis: 500 mg once a day, the duration of the course of therapy is 28 days;
- infections of the skin and soft tissues: 250-500 mg 1-2 times a day, the duration of the course of therapy is 7-14 days.
- drug-resistant forms of tuberculosis (as part of complex therapy): 500 mg 1–2 times a day, the duration of the course of therapy is up to 90 days.
For the treatment of patients with impaired renal function (CC 50–20 ml / min), correction of the dosage regimen is required.
Taking Leflobact tablets can be prescribed to continue the treatment started by using the drug in the form of an infusion solution.
Solution for infusion 0.5%
Leflobact solution is intended for slow intravenous drip. The infusion rate should correspond to the introduction of 100 ml of solution over 1 hour.
The dose is determined depending on the clinical indications, the severity of the infection and the susceptibility of the suspected pathogen to the drug.
Recommended dosage of Leflobact according to indications:
- community-acquired pneumonia: 100 ml (500 mg) 1-2 times a day, for 7-14 days;
- uncomplicated urinary tract infections: 50 ml once a day for 3 days;
- acute pyelonephritis and other complicated urinary tract infections: 50 ml once a day, for 7-10 days;
- infections of the skin and soft tissues: 100 ml 2 times a day for 7-14 days;
- chronic bacterial prostatitis: 100 ml once a day for 28 days;
- septicemia or bacteremia: 100 ml 1-2 times a day for 10-14 days;
- intra-abdominal infections (in combination with antibacterial agents acting on the anaerobic flora): 100 ml once a day for 7-14 days.
In case of impaired renal function, the dosage regimen is adjusted taking into account the patient's CC value and the usual dose for patients with normal renal function.
Additional administration of Leflobact after hemodialysis or prolonged peritoneal dialysis is not required.
If liver function is impaired, correction of the usual dosage regimen of Leflobact is not required.
After several days of intravenous administration of the drug and with positive dynamics of therapy, the patient can be transferred to taking pills in the same dose.
It is recommended to continue the use of Leflobact for another 2-3 days after reliable eradication of the pathogen and a decrease in body temperature.
Side effects
- from the hematopoietic system: hemolytic anemia, eosinophilia, leukopenia, thrombocytopenia, neutropenia, pancytopenia, agranulocytosis, hemorrhages;
- from the digestive system: nausea, vomiting, loss of appetite, diarrhea (in the case of tablets - including blood), abdominal pain, pseudomembranous colitis, dysbiosis, hyperbilirubinemia, hepatitis, increased activity of hepatic transaminases; in addition, when taken orally - indigestion, when using the solution - severe liver failure, acute liver failure, especially in cases of severe underlying disease (including sepsis);
- from the nervous system: weakness, drowsiness, headache, dizziness, insomnia, hallucinations, fear, paresthesia, confusion, movement disorders, anxiety or anxiety, tremors, depression, convulsions (with a predisposition for epileptic seizures); in addition, when using the solution - nightmares, peripheral neuropathy (sensory, sensorimotor), psychotic reactions, extrapyramidal disorders, self-injurious behavior with suicidal thoughts and actions, agitation;
- on the part of the cardiovascular system: lowering blood pressure (BP), tachycardia, vascular collapse, prolongation of the QT interval;
- from the musculoskeletal system: myasthenia gravis, arthralgia, myalgia, tendonitis, tendon rupture, rhabdomyolysis;
- on the part of the senses: hearing loss, impaired smell (parosmia), taste (ageusia, dysgeusia); in addition: when taken orally - visual impairment, tactile sensitivity; when using the solution - loss of smell, vertigo, ringing in the ears;
- from the side of metabolism: hypoglycemia (increased sweating, increased appetite, tremors); in addition, when using the solution - attacks of porphyria;
- from the urinary system: acute renal failure, hypercreatininemia, interstitial nephritis;
- from the immune system: itching, skin flushing, urticaria, edema (skin, mucous membranes), bronchospasm, dyspnea, Stevens-Johnson syndrome (malignant exudative erythema), Lyell's syndrome (toxic epidermal necrolysis), allergic pneumonitis, anaphylactic shock, vasculitis; in addition, when using the solution - shortness of breath;
- local reactions: when applying the solution - phlebitis, periphlebitis;
- others: persistent fever, photosensitivity, exacerbation of porphyria, asthenia, development of superinfection.
Overdose
Symptoms: dizziness, confusion, lengthening of the QT interval, seizures.
Treatment: the appointment of symptomatic therapy. Dialysis is ineffective.
special instructions
For the treatment of severe pneumonia caused by pneumococci, the clinical effect of Leflobact may be insufficient.
IV administration of the drug should be accompanied by blood pressure control, since in some cases a transient decrease in blood pressure and a feeling of heartbeat are possible. If the pressure drops significantly, the infusion should be stopped immediately.
During the treatment period, it is recommended to avoid exposure to direct sunlight and artificial ultraviolet radiation.
Concomitant use of drugs that cause prolongation of the QT interval increases the risk of developing cardiac arrhythmias.
If symptoms of allergic reactions, neuropathy, tendonitis or pseudomembranous colitis develop, the use of levofloxacin should be discontinued immediately.
During the period of treatment of patients with a history of brain damage, the possible development of seizures should be considered.
With a deficiency of glucose-6-phosphate dehydrogenase, the risk of hemolysis increases.
In case of impaired renal function, treatment should be accompanied by monitoring of renal function in order to correct the dosage regimen if necessary.
The use of alcohol is contraindicated during the entire period of therapy.
Influence on the ability to drive vehicles and complex mechanisms
During the period of Leflobact's use, one should not engage in potentially hazardous activities, the implementation of which requires quick psychomotor reactions and increased attention, including driving.
Application during pregnancy and lactation
The use of Leflobact is contraindicated during gestation and lactation.
If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued during the entire period of treatment.
Pediatric use
The use of levofloxacin for the treatment of patients under the age of 18 is contraindicated.
With impaired renal function
The use of Leflobact tablets for the treatment of patients with impaired renal function (CC less than 20 ml / min) and during hemodialysis is contraindicated.
In case of impaired renal function with CC 50–20 ml / min, the following dosage regimen is prescribed for taking the drug inside:
- clinical indications requiring the appointment of a daily dose of 500 mg: the first day - 500 mg, then 250 mg once a day;
- clinical indications requiring the appointment of a daily dose of 1000 mg: the first dose - 500 mg, then 250 mg with an interval of 12 hours.
When prescribing a solution for Leflobact infusion to patients with impaired renal function, correction of the dosage regimen is required. It is produced taking into account the patient's CC value and the usual dose for patients with normal renal function according to the following scheme:
- clinical indications requiring the appointment of a daily dose of 50 ml of solution (250 mg): the first dose - 50 ml (250 mg), then: with CC 50-20 ml / min - 25 ml once a day, with CC 19-10 ml / min - 25 ml 1 time in 2 days, with CC less than 10 ml / min, including hemodialysis and peritoneal dialysis - 25 ml 1 time in 2 days;
- clinical indications requiring the appointment of a daily dose of 100 ml of solution (500 mg): the first dose - 100 ml (500 mg), then: with CC 50-20 ml / min - 50 ml 1 time per day, with CC 19-10 ml / min - 25 ml once a day, with CC less than 10 ml / min, including hemodialysis and peritoneal dialysis - 25 ml once a day;
- clinical indications requiring the appointment of a daily dose of 200 ml (1000 mg): the first dose - 100 ml, then: with CC 50–20 ml / min - 50 ml (250 mg) 2 times a day, with CC 19–10 ml / min - 25 ml (125 mg) 2 times a day, with CC less than 10 ml / min, including hemodialysis and peritoneal dialysis - 25 ml 1 time per day.
Additional administration of Leflobact after hemodialysis or prolonged peritoneal dialysis is not required.
For violations of liver function
In case of impaired liver function, correction of the Leflobact dosage regimen is not required.
Use in the elderly
Care should be taken when treating elderly patients because of the high likelihood of decreased renal function in them.
Drug interactions
With simultaneous use with Leflobact:
- non-steroidal anti-inflammatory drugs from the ibuprofen group, theophylline: can increase the seizure threshold of levofloxacin;
- glucocorticosteroids: increase the risk of tendon rupture, especially in elderly patients;
- cimetidine, probenecid with cimetidine and drugs that block tubular secretion: cause a slight slowdown in the excretion of levofloxacin;
- cyclosporin: levofloxacin increases its T 1/2;
- warfarin, vitamin K antagonists: increases prothrombin time, increases the risk of bleeding;
- ethanol: enhances the side effects of the drug from the central nervous system (drowsiness, dizziness);
- oral hypoglycemic agents, insulin: require careful monitoring of blood glucose concentration due to the risk of developing hypo- and hyperglycemic conditions;
- antiarrhythmic drugs (class IA, III), antipsychotics, tetracyclic and tricyclic antidepressants, imidazole derivatives, antifungal agents, macrolides, antihistamines (including astemizole, ebastine, terfenadine): increase the risk of prolongation of the QT interval.
It is recommended to observe a break of at least two hours between oral administration of Leflobact and the following concomitant therapy drugs: drugs that have a depressing effect on intestinal motility, aluminum and magnesium-containing antacids, sucralfate, iron salt preparations.
Solution for infusion Leflobact can be mixed with 0.9% sodium chloride solution, 2.5% Ringer's solution with dextrose, 5% dextrose (glucose) solution, combined solutions for parenteral nutrition (carbohydrates, amino acids, electrolytes).
Do not mix levofloxacin solution with solutions that are alkaline, heparin.
Analogs
Lefloxacin analogs are Levofloxacin, Abaktal, Zanocin, Zoflox, Glevo, Gatifloxacin, Lebel, Levolet, Levostar, Levoflox, Lomflox, Lefokcin, Maklevo, Moxifloxacin, Tsiprobai, Sparflo, Pefloxacin, Remedionf, Schaifloks, Eigerliflox, Tariflvid, Faktiv, etc.
Terms and conditions of storage
Keep out of the reach of children.
Storage conditions: tablets - at temperatures up to 25 ° C in a place protected from moisture and light; infusion solution - at a temperature of 15-25 ° C in a dark place, avoid freezing.
Shelf life: tablets - 3 years; infusion solution - 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Leflobact
In reviews of Leflobact, patients give a positive assessment of the therapeutic efficacy of the drug for many diseases of bacterial etiology, including pathologies of the urogenital tract and the respiratory system. The rather low cost of tablets and solution is often noted, comparing it with other antibacterial drugs.
The disadvantages include the development against the background of the use of levofloxacin of such undesirable phenomena as headache, dizziness, palpitations, with prolonged use - muscle pain.
Price for Leflobact in pharmacies
The approximate price for Leflobact for a package containing 10 tablets at a dose of 250 mg can be from 37 rubles, at a dose of 500 mg - from 70 rubles, for 1 bottle of solution - from 34 rubles.
Leflobact: prices in online pharmacies
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Drug name Price Pharmacy |
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Leflobact 500 mg film-coated tablets 5 pcs. 139 RUB Buy |
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Leflobact 5 mg / ml solution for infusion 100 ml 1 pc. 199 RUB Buy |
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Leflobact 250 mg film-coated tablets 10 pcs. 201 RUB Buy |
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Leflobact tablets p.p. 500mg 5 pcs. 208 RUB Buy |
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Leflobact 500 mg film-coated tablets 10 pcs. 367 r Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
