Lebel tablets p/o 750 mg No. 7x1
Name
Lebel.
Release forms
Pills.
INN
Levofloxacin.
FTG
Antimicrobial agent; fluoroquinolone.
Compound
1 film-coated tablet contains: active substance: levofloxacin hemihydrate, equivalent to 500 mg or 750 mg of levofloxacin; excipients: microcrystalline cellulose PH 102, hydroxypropyl methylcellulose (Pharmacout 603 W), crospovidone (Kollidon Cl), sodium stearyl fumarate, film coating: Opadry Y1 7000 white. Composition of film shell material No. 8 (Opadray Y1 7000 white): hypromellose (HPMC 5 cP-methocel E5-LV), titanium dioxide (E171), polyethylene glycol (PEG 400).
Description
White or almost white oblong tablets, 500 mg, with rounded ends, film-coated, scored on one side. The tablet can be divided into equal halves. White or off-white oblong tablets, 750 mg, with rounded ends, film-coated.
Pharmacotherapeutic group
Antibacterial agents for systemic use. Antibacterial agents, quinolone derivatives. Fluoroquinolones. ATX code: J01MA12.
Indications for use
Lebel® is indicated in adults for the treatment of the following infections: • Acute bacterial sinusitis • Exacerbation of chronic bronchitis • Community-acquired pneumonia • Complicated skin and soft tissue infections • Uncomplicated acute cystitis For the treatment of the above infections, levofloxacin should be used only when it is considered inappropriate to use antibacterial agents that are usually recommended for the initial treatment of these infections. • Acute pyelonephritis and complicated urinary tract infections • Chronic bacterial prostatitis • Inhalation anthrax: post-exposure prophylaxis and for radical treatment. Lebel® may also be used to complete a course of therapy in patients who have shown improvement during initial treatment with intravenous levofloxacin. Official recommendations for the appropriate use of antibacterial agents should be taken into account.
Directions for use and doses
Lebel® film-coated tablets are taken once or twice a day. The dose depends on the type and severity of infection and the susceptibility of the suspected pathogen. Lebel® tablets can also be used for complex therapy in patients who have improved during the initial stage of treatment with intravenous levofloxacin, given the bioequivalence of the parenteral and oral forms, the same dose can be used. The following doses are recommended for Lebel®: Doses for patients with normal renal function (creatinine clearance >50 ml/min) Indication Dose Duration of treatment (according to severity) (according to severity) Acute bacterial sinusitis 500 mg once daily 10-14 days 750 mg once a day 5 days Exacerbation of chronic bronchitis 500 mg once a day 7-10 days Community-acquired pneumonia 500 mg once or twice a day* 7-14 days 750 mg once a day** 5 days Acute pyelonephritis 500 mg once daily for 7-10 days Complicated urinary tract infections 500 mg once daily for 7-14 days Uncomplicated acute cystitis 250 mg once daily for 3 days Chronic bacterial prostatitis 500 mg once daily for 28 days Complicated infections skin and soft tissue 500 mg once or twice daily 7-14 days 750 mg once daily Pneumonic anthrax 500 mg once daily 8 weeks * – caused by methicillin-susceptible Staphylococcus aureus, Streptococcus pneumoniae (including isolates with multiple drug resistance
MDRSP
), Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Chlamydophila pneumoniae, Legionella pneumophila or Mycoplasma pneumoniae; ** – caused by Streptococcus pneumoniae (except for multidrug-resistant isolates
MDRSP
), Haemophilus influenzae, Haemophilus parainfluenzae, Mycoplasma pneumoniae or Chlamydophila pneumoniae. Special groups: Doses for patients with impaired renal function (creatinine clearance ≤ 50 ml/min) Dosage regimen 250 mg/24 hours 500 mg/24 hours 500 mg/12 hours Creatinine clearance First dose: 250 mg First dose: 500 mg First dose: 500 mg 50-20 ml/min. Then 125 mg/24 hours Then 250 mg/24 hours Then 250 mg/12 hours 19-10 ml/min. Then 125 mg/48 hours Then 125 mg/24 hours Then 125 mg/12 hours
Mode of application
Lebel® tablets should be swallowed without crushing with sufficient liquid. Lebel® 500 mg, film-coated tablets can be divided according to risk to adapt the dose. The tablets can be taken with or before meals. Lebel® tablets are taken at least 2 hours before or 2 hours after taking iron salts, zinc, magnesium/aluminum antacids, or didanosine (only didanosine compounds with aluminum or magnesium containing buffer substances) and sucralfate, as a decrease in absorption. If you miss a dose of the drug, you should take the pill as soon as possible before the time for your next dose approaches. Then continue taking Lebel® according to the recommended regimen. Do not double the dose for the missed dose. Patients receiving Lebel® should maintain adequate fluid intake to prevent the formation of highly concentrated urine and the development of crystalluria and cylindruria, which have been reported during treatment with quinolones.
Contraindications
• Hypersensitivity to levofloxacin, other quinolones and excipients included in the drug (see section “Composition”). • Tendon lesions due to previous fluoroquinolone treatment. • Pregnancy, lactation period. • Childhood and adolescence (up to 18 years). • Epilepsy. With caution: old age, glucose-6-phosphate dehydrogenase deficiency.
Side effect
Like all medicines, Lebel® can cause side effects, although not everyone gets them. Stop taking Lebel® and call your doctor or hospital immediately if you notice the following side effects: Very rare (may affect less than 1 in 10,000 people): Allergic reaction. Signs may include: rash, problems swallowing and breathing, swelling of the lips, face, throat or tongue. Stop taking Lebel and call your doctor immediately if you notice any of the following serious side effects - You may need urgent medical attention: Rare (may affect less than 1 in 1000 people): Watery diarrhea, which may contain blood, possibly with stomach cramps and high fever. This could be a sign of a serious bowel problem. Pain and inflammation in tendons or ligaments, which may lead to rupture. The Achilles tendon is most commonly affected. Seizures (convulsions). Very rare (may affect less than 1 in 10,000 people): Burning, tingling, pain or numbness. These may be signs of a condition called neuropathy. Others: Common skin rashes, which may include blistering or peeling of the skin around the lips, eyes, mouth, nose, and genitals. Loss of appetite, yellow skin and eyes, dark urine, itching or pain in the stomach (abdomen). These may be signs of liver problems, including fatal liver failure. If there is blurred vision or any other visual disturbances while taking Lebel®, contact your eye doctor immediately. The following undesirable reactions have also been reported: Common - may occur in less than 1 in 10 people: sleep problems, headache, dizziness, nausea, vomiting and diarrhea, increased activity of certain liver enzymes in the blood. Uncommon – may affect less than 1 in 100 people: • changes in the number of bacteria or fungi, infection with a fungus called Candida; • changes in the number of leukocytes detected as a result of certain blood tests (leukopenia, eosinophilia); • feeling of stress (anxiety), confusion, nervousness, drowsiness, trembling, vertigo; • lack of air (shortness of breath); • loss of taste, loss of appetite, upset stomach or indigestion (dyspepsia), abdominal pain, feeling of bloating (flatulence) or constipation; • itching and skin rashes, severe itching or hives, excessive sweating (hyperhidrosis); • joint pain or muscle pain; • blood tests may show unusual results due to problems with the liver (increased bilirubin) or kidney problems (increased creatinine); • general weakness. Rare - may affect less than 1 in 1,000 people: • easy bruising and bleeding due to low platelet counts (thrombocytopenia); • low white blood cell count (neutropenia); • hyperactive immune response (hypersensitivity); • decreased blood sugar levels (hypoglycemia). This is important for people with diabetes. • hallucinations, paranoia, changes in opinion and thoughts (psychotic reactions) with a risk of suicidal thoughts or actions; • feelings of depression, mental problems, anxiety (excitement), abnormal dreams or nightmares; • tingling sensation in the arms and legs (paresthesia); • problems with hearing (tinnitus) or vision (blurred vision); • unusually fast heartbeat (tachycardia) or low blood pressure (hypotension); • muscle weakness. This is important for people with myasthenia gravis (a rare disease of the nervous system). • changes in kidney function and kidney failure, which may be associated with an allergic kidney reaction called interstitial nephritis. • fever. Others: • low levels of red blood cells (anemia): this can make the skin pale or yellow due to damage to the red blood cells; decrease in the number of all types of blood cells (pancytopenia); • fever, sore throat and a general feeling of malaise that does not go away. This may be due to a decrease in the number of white blood cells (agranulocytosis). • decreased blood circulation (pseudo-anaphylactic shock); • increased blood sugar (hyperglycemia) or decreased blood sugar leading to coma (hypoglycemic coma). This is important for people with diabetes. • loss of smell or taste (parosmia, anosmia, ageusia); • problems with movement and walking (dyskinesia, extrapyramidal disorders); • temporary loss of consciousness or fainting; • temporary loss of vision; • hearing impairment or loss; • abnormal fast heart rhythm, life-threatening irregular heart rhythm, including cardiac arrest, changes in heart rhythm (so-called “QT prolongation” seen on ECG, electrical activity of the heart); • difficulty breathing or shortness of breath (bronchospasm); • allergic reactions of the lungs; • pancreatitis; • inflammatory liver diseases (hepatitis); • increased skin sensitivity to the sun and ultraviolet radiation (photosensitivity); • inflammation of blood vessels (vasculitis); • inflammation of the mucous membrane in the mouth (stomatitis); • muscle rupture and muscle destruction (rhabdomyolysis); • redness and swelling of the joints (arthritis); • pain, including pain in the back, chest and limbs; • attacks of porphyria in patients already suffering from this disease (a very rare metabolic disease); • persistent headache with or without blurred vision (idiopathic intracranial hypertension). Very rare cases of long-term (up to several months or years) or persistent adverse reactions such as tendon inflammation, tendon rupture, joint pain, limb pain, difficulty walking, abnormal sensations such as tingling, tickling, burning, numbness or pain (neuropathy), depression, fatigue, sleep disturbances, memory impairment, and impairment of hearing, vision, taste and smell have been associated with quinolone- and fluoroquinolone-containing antibiotics, sometimes regardless of the presence of existing risk factors. Reporting Adverse Reactions If you experience any adverse reactions, you are advised to consult your doctor. This recommendation applies to any possible adverse reactions, including those not listed in the package insert. You can also report adverse reactions to the Adverse Drug Events Information Database, including reports of drug failure. By reporting adverse reactions, you can help provide more information about the safety of the drug.
Interaction with other drugs and food products
The influence of other drugs on levofloxacin Iron salts, zinc salts, magnesium- or aluminum-containing antacids, didanosine The absorption of levofloxacin is significantly reduced when concomitantly taken with Lebel® tablets iron salts, magnesium- or aluminum-containing antacids, didanosine (only drugs with didanosine containing as buffer substances aluminum or magnesium). Taking fluoroquinolones with multivitamins containing zinc appears to reduce their oral absorption. Medicines containing divalent or trivalent cations, such as iron salts, zinc salts or antacids containing magnesium or aluminum, or didanosine (only didanosine preparations containing aluminum or magnesium as buffering agents) are recommended to be taken at least 2 hours before or after taking Lebel® tablets. Calcium salts have a minimal effect on the oral absorption of levofloxacin. Sucralfate The bioavailability of Lebel® tablets is significantly reduced when taken together with sucralfate. If patients must take sucralfate and Lebel®, it is recommended that sucralfate be taken 2 hours after taking Lebel® tablets. Theophylline, fenbufen or similar non-steroidal anti-inflammatory drugs Pharmacokinetic interactions of levofloxacin with theophylline were not detected in a clinical study. However, when quinolones are used in combination with theophylline, nonsteroidal anti-inflammatory drugs, or other drugs that lower the seizure threshold, a significant decrease in the seizure threshold may be observed. Concentrations of levofloxacin in the presence of fenbufen increased by 13% compared with the concentration when taking levofloxacin alone. Probenecid and cimetidine Probenecid and cimetidine had a statistically significant effect on the elimination of levofloxacin. Renal clearance of levofloxacin was reduced by cimetidine (24%) and probenecid (34%). This is due to the fact that both drugs are able to block the secretion of levofloxacin in the renal tubules. However, given the doses used in the study, it is unlikely that this statistically significant kinetic difference would be clinically significant. Caution should be exercised when levofloxacin is co-administered with drugs that affect renal tubular secretion, such as probenecid and cimetidine, especially in patients with impaired renal function. Other relevant information Studies of the pharmacological properties in clinical use have shown that the pharmacokinetics of levofloxacin were not affected to any clinically significant extent when levofloxacin was used in conjunction with the following drugs: calcium carbonate, digoxin, glibenclamide, ranitidine. Effect of levofloxacin on other drugs Cyclosporine The half-life of cyclosporine increases by 33% when administered simultaneously with levofloxacin. Vitamin K antagonists In patients receiving levofloxacin in combination with a vitamin K antagonist (eg, warfarin), there was an increase in coagulation test results (PT/MHO) and/or bleeding, up to severe. In this regard, in patients receiving vitamin K antagonists, it is necessary to monitor the results of a coagulation test. Drugs Known to Prolong the QT Interval Levofloxacin, like other fluoroquinolones, should be used with caution in patients receiving drugs known to prolong the QT interval (e.g., Class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, antipsychotics). Other relevant information In a pharmacokinetic interaction study, levofloxacin had no effect on the pharmacokinetics of theophylline (which is a marker substrate of CYP1A2), indicating that levofloxacin is not an inhibitor of CYP1A2. Other types of interactions Food There is no clinically significant interaction with food. Thus, Lebel® tablets can be taken regardless of meals. Effect on laboratory tests In patients treated with levofloxacin, the determination of opiates in urine may give false-positive results. It may be necessary to confirm positive test results with a more specific method. Levofloxacin may inhibit the growth of Mycobacterium tuberculosis and, therefore, give false-negative results in the bacteriological diagnosis of tuberculosis.
Precautionary measures
Before taking this medicine You should not take fluoroquinolone/quinolone antibacterial drugs, including Lebel®, if you have experienced any serious adverse reactions while taking a quinolone or fluoroquinolone in the past. In this situation, you should inform your doctor as soon as possible. Long-lasting, disabling and potentially irreversible serious side effects Fluoroquinolone/quinolone antibacterial drugs, including levofloxacin, have been associated with very rare but serious side effects. some of which were long-term (lasting months or years), disabling, or potentially irreversible. These include tendon rupture, muscle and joint pain in the upper and lower extremities, difficulty walking, abnormal sensations such as tingling, tickling, numbness or burning (paresthesia), sensory disturbances including impairment of vision, taste and smell, hearing, depression, memory loss, extreme fatigue and severe sleep disturbances. If you experience any of these side effects after taking Lebel®, contact your doctor immediately before continuing treatment. You and your doctor will decide whether to continue treatment, also considering an antibiotic from a different class. Tendonitis and tendon rupture While taking this drug, you may have pain and swelling in your joints, and inflammation or rupture of your tendons. Your risk increases if you are older (over 60 years old), have had an organ transplant, have kidney problems, or are being treated with corticosteroids. Inflammation and tendon ruptures may occur within the first 48 hours of treatment and even for several months after stopping therapy. At the first sign of tendon pain or inflammation (for example, in the ankle, wrist, elbow, shoulder, or knee), stop taking Lebel®, call your doctor, and immobilize the painful area. Avoid any unnecessary exercise as this may increase the risk of tendon rupture. Peripheral neuropathy You may rarely experience symptoms of nerve damage (neuropathy), such as pain, burning, tingling, numbness and/or weakness, especially in the feet and legs or arms and hands. If this happens, stop taking Lebel® Tablets and tell your doctor immediately to prevent a potentially irreversible condition from developing. Central nervous system disorders Adverse reactions from the central nervous system during treatment with fluoroquinolones. including levofloxacin, were associated with an increased risk of seizures, increased intracranial pressure (including pseudotumor cerebri), tremor and dizziness. As is the case with other fluoroquinolones. Levofloxacin should be used with caution in patients with a known or suspected central nervous system (CNS) disorder that may predispose them to seizures or lower the seizure threshold (eg, severe cerebral atherosclerosis) or in the presence of other risk factors that may predispose them to seizures or lower the seizure threshold (eg, some drug therapy, renal dysfunction). If these reactions occur in patients receiving levofloxacin, treatment with Lebel® should be discontinued and appropriate measures taken. Psychiatric disorders Fluoroquinolones, including levofloxacin, have been associated with an increased risk of psychiatric adverse reactions, including: toxic psychosis, hallucinations or paranoia; depression or thoughts of suicide; anxiety, agitation, restlessness or nervousness; confusion, delirium, disorientation, or disturbances in attention; insomnia or nightmares; memory impairment. Attempted or completed suicide has been reported, especially in patients with a history of depression or risk factors for depression. These reactions may occur after the first dose. If these reactions occur in patients receiving levofloxacin, treatment should be discontinued and appropriate measures taken. Methicillin-resistant S. aureus is likely to be co-resistant to fluoroquinolones. including levofloxacin. Therefore, levofloxacin is not recommended for the treatment of known or suspected MRSA infections. if laboratory results do not confirm the body's susceptibility to levofloxacin (and conventional antibacterial drugs for the treatment of MRSA infections are considered unsuitable). Levofloxacin can be used to treat acute bacterial sinusitis and exacerbation of chronic bronchitis if these infections have been properly diagnosed. Fluoroquinolone resistance in E. coli, the most common causative agent of urinary tract infections, varies across the European Union. Clinicians are advised to consider the local prevalence of fluoroquinolone resistance in E. coli. Inhalational anthrax: use in humans is based on in vitro susceptibility data for Bacillus anthracis and experimental data in animals, as well as limited data in humans. Prescribers should refer to national and/or international consensus documents regarding the treatment of anthrax. Clostridium difficile-associated disease Diarrhea, especially severe, persistent and/or bloody, that occurs during or after treatment with levofloxacin (including several weeks after treatment) may be a symptom of Clostridium difficile-associated disease (CDAD). CDAD can range in severity from mild to life-threatening, the most severe form of which is pseudomembranous colitis. Therefore, it is important to consider this diagnosis in patients who develop severe diarrhea during or after treatment with levofloxacin. If CDAD is suspected or confirmed, levofloxacin should be discontinued immediately and appropriate treatment initiated without delay. Drugs that inhibit peristalsis are contraindicated in this clinical situation. Patients with G6-phosphate dehydrogenase deficiency Patients with latent or overt defects in glucose-6-phosphate dehydrogenase activity may be susceptible to hemolytic reactions when treated with quinolone antibacterial drugs. Therefore, if levofloxacin is to be used in these patients, the potential occurrence of hemolysis should be monitored. Patients with renal impairment Since levofloxacin is eliminated primarily by the kidneys, the dose of Lebel® should be adjusted in patients with renal impairment. Hypersensitivity reactions Levofloxacin may cause serious or fatal hypersensitivity reactions (eg, angioedema and anaphylactic shock), including after the first dose. Patients should stop treatment immediately and contact a physician or emergency physician, who will take appropriate emergency measures. Severe bullous reactions Cases of severe bullous skin reactions have been reported with the use of levofloxacin, such as Stevens-Johnson syndrome or toxic epidermal necrolysis. Patients should consult a doctor immediately before continuing treatment if skin and/or mucous membrane reactions occur. Dysglycemia As with all quinolones, disturbances of blood glucose levels, including hypoglycemia and hyperglycemia, have been observed, usually in diabetic patients receiving concomitant therapy with oral hypoglycemic agents (eg, glibenclamide) or insulin. Cases of hypoglycemic coma have been reported. For such patients, careful monitoring of blood glucose levels is recommended. Prevention of photosensitivity Although photosensitization is very rare with the use of levofloxacin, to avoid it, patients are advised not to unnecessarily expose themselves to strong sunlight or artificial ultraviolet radiation during treatment and for 48 hours after stopping treatment (for example, sun exposure in highlands or visiting a solarium). Liver failure Cases of liver necrosis up to life-threatening conditions have been reported, especially in patients with severe pre-existing diseases, such as sepsis. Patients should stop treatment and consult a doctor if signs and symptoms of liver disease develop, such as anorexia, jaundice, dark urine, itching, or tenderness to the abdomen. Exacerbation of myasthenia gravis Fluoroquinolones, including levofloxacin, have neuromuscular blocking activity and may exacerbate muscle weakness in patients with myasthenia gravis. Severe adverse reactions reported in post-marketing experience, including deaths and the need for mechanical ventilation, have been associated with the use of fluoroquinolones in patients with myasthenia gravis. Levofloxacin is not recommended for patients with a history of myasthenia gravis. Visual disturbances If you have visual disturbances or if any effects on the organ of vision occur, you should immediately consult an ophthalmologist. Superinfection The use of levofloxacin, especially long-term, can lead to excessive growth of microorganisms that are insensitive to it. If superinfection develops during therapy, appropriate measures should be taken. Cardiovascular disorders QT prolongation Caution should be exercised when using fluoroquinolones, including levofloxacin, in patients with known risk factors for QT prolongation, such as: - congenital long QT syndrome; - concomitant use of drugs that are known to prolong the QT interval (for example, class IA and III antiarrhythmic drugs, tricyclic antidepressants, macrolides, antipsychotic drugs); - disturbed electrolyte balance (for example, hypokalemia, hypomagnesemia); - heart disease (for example, heart failure, myocardial infarction, bradycardia). Elderly patients and women may be more sensitive to drugs that prolong the QT interval. Therefore, caution should be used when using fluoroquinolones, including levofloxacin, in these patients. Development of aneurysm and aortic dissection There is information about an increased risk of developing aneurysm and aortic dissection after the use of fluoroquinolones, especially in elderly patients. Before you start using Lebel® tablets, tell your doctor if you have the following conditions: - if you have been diagnosed with an enlargement or "dilation" of a large blood vessel (aortic aneurysm or peripheral large vessel aneurysm) - if you have previously had an episode of aortic dissection (rupture of the aortic wall) - if you have a history of aortic aneurysm or dissection, or other risk factors or predisposing conditions (for example, connective tissue diseases such as Marfan syndrome, vascular Ehlers-Danlos syndrome, Takayasu arteritis, giant cell arteritis, Behçet's disease, hypertension, atherosclerosis). If patients experience sudden pain in the abdomen, chest, or back, they should contact their doctor immediately at the emergency room.
Fertility, pregnancy and lactation
Pregnancy There is limited data on the use of levofloxacin in pregnant women. Animal studies do not indicate direct or indirect harmful effects in terms of reproductive toxicity. However, due to the lack of human data and experimental data suggesting that fluoroquinolones may cause damage to growing cartilage, levofloxacin should not be taken by pregnant women. Breastfeeding Lebel® is contraindicated in nursing women. There is insufficient information about the excretion of levofloxacin into milk. However, other fluoroquinolones pass into breast milk. In the absence of human data and because experimental evidence suggests that fluoroquinolones may cause damage to growing cartilage, levofloxacin should not be used in breastfeeding women. Fertility Levofloxacin did not cause impairment of fertility or reproductive function in rats.
Impact on the ability to drive vehicles and operate machinery
Adverse effects such as dizziness, drowsiness, and visual disturbances may impair the patient's ability to concentrate and react, which may pose a risk in situations where these abilities are of particular importance (for example, driving or operating machinery).
Overdose
According to animal toxicity studies or clinical pharmacological studies performed at supra-therapeutic doses, the most important signs to be expected after an acute overdose of Lebel® tablets are central nervous system symptoms such as confusion, dizziness, impaired consciousness and seizures, QT prolongation, and gastrointestinal reactions such as nausea and mucosal erosion. CNS effects, including confusion, seizures, hallucinations, and tremors, have been observed post-marketing. In case of overdose, symptomatic treatment should be carried out. Due to the risk of QT prolongation, ECG monitoring should be performed. Taking antacids can be used to protect the stomach lining. Hemodialysis, including peritoneal dialysis and chronic ambulatory peritoneal dialysis, is not effective in removing levofloxacin from the body. There is no specific antidote.
Storage conditions
Store at a temperature not exceeding 25°C. Keep away from children!
Conditions for dispensing from pharmacies
On prescription.
Best before date
4 years. Do not use after the expiration date indicated on the package.
Package
7 tablets of 500 mg, film-coated, in blister packaging made of PVC/PE/HDPE/aluminum. 1 strip packaging with instructions for use in a cardboard box. 7 tablets of 750 mg, film-coated, in blister packaging made of PVC/PE/HDPE/aluminum. 1 strip packaging with instructions for use in a cardboard box.
Buy Lebel tablet. p/o 750 mg per cont. cell pack No. 7x1 in the pharmacy
Price for Lebel table. p/o 750 mg per cont. cell pack No. 7x1
Instructions for use for Lebel tablet. p/o 750 mg per cont. cell pack No. 7x1
Lebel
Fluoroquinolone, a broad-spectrum antimicrobial bactericidal agent. Blocks 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 bacteria.
In vitro activity:
Sensitive microorganisms (minimum inhibitory concentration less than 2 mg/l).
Aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (coagulase-negative methicillin-sensitive/moderately sensitive strains), including Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis (methicillin-sensitive strains), Staphylococcus spp. (leukotoxin-containing); Streptococcus spp. groups C and G, Streptococcus agalactiae, Streptococcus pneumoniae (penicillin-sensitive/moderately sensitive/resistant strains), Streptococcus pyogenes, Streptococcus viridans group (penicillin-sensitive/resistant strains).
Aerobic gram-negative microorganisms: Acinetobacter spp. (including Acinetobacter baumannii), Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter spp. (including Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (ampicillin-sensitive/resistant strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella catarrhalis (beta-lactamase producing and non-producing strains), Morganella morganii, Neisseria gonorrhoeae (penicillinase producing and non-producing strains), Neisseria meningitidis, Pasteurella spp. (including Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (including Pseudomonas aeruginosa), Serratia spp. (including Serratia marcescens), Salmonella spp.
Anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterium spp., Veilonella spp.
Dr. microorganisms: Bartonella spp., Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella spp. (including Legionella pneumophila), Mycobacterium spp. (including Mycobacterium leprae, Mycobacterium tuberculosis, Mycoplasma hominis), Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum.
Moderately sensitive microorganisms (minimum inhibitory concentration more than 4-8 mg/l):
Aerobic gram-positive microorganisms: Corynebacterium urealyticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis (methicillin-resistant strains), Staphylococcus haemolyticus (methicillin-resistant strains).
Aerobic gram-negative microorganisms: Burkholderia cepacia, Campylobacter jejuni, Campylobacter coli.
Anaerobic microorganisms: Bacteroides thetaiotaomicron, Bacteroides vulgatus, Bacteroides ovatus, Prevotella spp., Porphyromonas spp.
Resistant microorganisms (minimum inhibitory concentration more than 8 mg/l):
Aerobic gram-positive microorganisms: Corynebacterium jeikeium, Staphylococcus aureus (methicillin-resistant strains), other Staphylococcus spp. (coagulase-negative methicillin-resistant strains).
Aerobic gram-negative microorganisms: Alcaligenes xylosoxidans.
Dr. microorganisms: Mycobacterium avium.
Lebel, 500 mg, film-coated tablets, 7 pcs.
Nosocomial infections caused by Pseudomonas aeruginosa
), may require combination therapy.
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 if laboratory tests have not confirmed the sensitivity of this microorganism to levofloxacin.
Patients predisposed to developing seizures
Like other quinolones, levofloxacin should be used with great caution in patients with a predisposition to seizures. Such patients include patients with previous CNS lesions, such as stroke, severe traumatic brain injury; patients simultaneously receiving 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").
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
Rarely observed, tendonitis with quinolones, including levofloxacin, can lead to rupture of tendons, including the Achilles tendon. This side effect can develop within 48 hours after starting treatment and can be bilateral. Elderly patients are more prone to developing tendonitis. The risk of tendon rupture may be increased when taking corticosteroids concomitantly. If tendonitis is suspected, treatment with Lebel® should be stopped immediately and appropriate treatment of the affected tendon should be initiated, for example by providing sufficient immobilization (see sections “Contraindications” and “Side Effects”).
Hypersensitivity reactions
Levofloxacin may 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
Cases of severe bullous skin reactions such as Stevens-Johnson syndrome or toxic epidermal necrolysis have been observed while taking levofloxacin (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 hepatic necrosis, including the development of 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 kidney failure
Since levofloxacin is excreted mainly by 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 borne in mind that patients in this group often have impaired renal function (see section “Dosage and Administration”).
Preventing the development of photosensitivity reactions
Although photosensitivity with levofloxacin is very rare, to prevent its development, patients are not recommended to be unnecessarily exposed to strong sunlight or artificial ultraviolet radiation (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, which can lead to the development of superinfection . 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 receiving 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”, “Overdose” and “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 hypoglycemia and hyperglycemia have been observed with the use of levofloxacin, usually in patients with diabetes mellitus receiving concomitant treatment with oral hypoglycemic drugs (for example, glibenclamide) or insulin preparations. Cases of hypoglycemic coma have been reported. In patients with diabetes mellitus, careful monitoring of blood glucose concentrations is required (see section "Side effects").
Peripheral neuropathy
Sensory and sensorimotor peripheral neuropathy, which may have a rapid onset, has been reported in patients receiving fluoroquinolones, including levofloxacin. If the patient develops symptoms of neuropathy, levofloxacin should be discontinued. This minimizes the possible risk of developing irreversible changes.
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 data on the sensitivity of Bacillus anthracis
based on
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
With the use of quinolones, including levofloxacin, the development of psychotic reactions has been reported, which in very rare cases progressed to the development of suicidal thoughts and behavior 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. 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.
Impact on the ability to drive vehicles and machinery
Caution should be exercised when driving or engaging in other potentially hazardous activities, as some side effects of levofloxacin, such as dizziness, drowsiness and visual disturbances, may adversely affect the ability to drive or perform potentially hazardous activities that require increased alertness. and speed of psychomotor reactions.
