Remedia, 5 pcs., 500 mg, film-coated tablets
Remedia is an antimicrobial drug from the group of fluoroquinolones, a levorotatory isomer of ofloxacin. Has a wide spectrum of antimicrobial action. Levofloxacin blocks DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA breaks, inhibits DNA synthesis, and causes profound morphological changes in the cytoplasm, cell wall and membranes of bacteria. Levofloxacin is active against most strains of microorganisms both in vitro and in vivo.
In vitro, sensitive (MIC < 2 mg/l) aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (coagulase-negative methicillin-sensitive/methicillin-moderately sensitive strains), Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis (methicillin-sensitive strains), Staphylococcus spp. (leukotoxin-containing and coagulase-negative methicillin-sensitive/moderately sensitive strains), Streptococcus spp. groups C and G (including Streptococcus agalactiae, Streptococcus pneumoniae (penicillin-sensitive/moderately sensitive/resistant strains), Streptococcus pyogenes, Streptococcus spp. viridans group (penicillin-sensitive/resistant strains); aerobic gram-negative microorganisms: Acinetobacter baumannii , 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 (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. (incl. Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia rettgeri, Providencia stuiartii), Pseudomonas spp. (including Pseudomonas aeruginosa), Salmonella spp., Serratia spp. (Serratia marcescens); anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterum spp., Veillonella spp.; other microorganisms: Bartonella spp., Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella pneumophila, Legionella spp., Mycobacterium spp. (including Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma hominis, Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum.
Levofloxation is moderately active (MIC>4 mg/l) against 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 thetaiotaomiсron, Bacteroides vulgatus, Bacteroides ovatus, Prevotella spp., Porphyromonas spp.
Aerobic gram-positive microorganisms are resistant to levofoloxacin (MIC > 8 mg/h): Corynebacterium jeikeium, Staphylococcus aureus (methicillin-resistant strains), Staphylococcus spp. (coagulase-negative methicillin-resistant strains); aerobic gram-negative microorganisms: Alcaligenes xylosoxidans; other microorganisms: Mycobacterium avium.
Pharmacokinetics
Distribution
Protein binding - 30-40%. Cumulation when prescribing a dose of 500 mg 1 time / day is insignificant. When prescribed at a dose of 500 mg 2 times / day, a slight accumulation may be observed. Css are achieved 3 days after the start of application.
Penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, urinary system organs, genitals, bone tissue, prostate gland, polymorphonuclear leukocytes, alveolar macrophages. Levofloxacin penetrates poorly into the cerebrospinal fluid.
The average concentrations in urine 8-12 hours after a single dose of 150, 300 or 500 mg of levofloxacin were 44, 91 and 200 g/l, respectively.
Metabolism
In the liver, a small portion of levofloxacin is metabolized to desmethyllevofloxacin and levofloxacin-N-oxide, which constitute <5% of levofloxacin excreted by the kidneys.
Removal
After administration in a single dose of 500 mg, T1/2 is 6-8 hours. It is excreted from the body mainly by the kidneys by glomerular filtration and tubular secretion. Less than 5% of levofloxacin is excreted as metabolites. 70% is excreted unchanged and 87% within 48 hours.
Remedia 500 mg 10 pcs. film-coated tablets
pharmachologic effect
Broad-spectrum antimicrobial agent, fluoroquinolone.
Acts bactericidal. Blocks DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA breaks, inhibits DNA synthesis, causes profound morphological changes in the cytoplasm, cell wall and membranes. Active against Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes and Streptococcus agalactiae, Viridans group streptococci, Enterobacter cloacae, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter sakazakii, Escherichia coli, Haemophilus influenzae , Haemophilus parainfluenzae, Klebsiella pneumoniae, Klebsiella oxytoca, Legionella pneumoniae, Moraxella catarrhalis, Proteus mirabilis, Pseudomonas aeruginosa, Pseudomonas fluorescens, Chlamydia pneumoniae, Mycoplasma pneumoniae, Acinetobacter anitratus, Acinetobacter baumannii, Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter diversus, Citrobacter freundii, Morganella morganii, Proteus vulgaris, Providencia rettgeri, Providcncia stuartii, Serratia marcescens, Clostridium perfringens.
Composition and release form Remedia 500 mg 10 pcs. film-coated tablets
Tablet - 1 tablet:
- Active substance: levofloxacin (in the form of hemihydrate) 500 mg;
- Excipients: microcrystalline cellulose, povidone K-30, crospovidone, colloidal silicon dioxide, magnesium stearate, sodium lauryl sulfate;
- shell composition: yellow film coating substance (hypromellose, talc, titanium dioxide, yellow iron oxide dye), propylene glycol.
10 tablets in a blister pack made of PVDC film and aluminum foil. 1 blister pack along with instructions for use in a cardboard box.
Description of the dosage form
Oblong, biconvex, yellow film-coated tablets with a score line on one side.
Directions for use and doses
For sinusitis - orally, 500 mg 1 time / day; for exacerbation of chronic bronchitis - 250-500 mg 1 time / day. For pneumonia - orally, 250-500 mg 1-2 times a day. (500-1000 mg/day). For urinary tract infections - orally, 250 mg 1 time / day. For infections of the skin and soft tissues - 250-500 mg orally 1-2 times a day.
For kidney diseases, the dose is reduced in accordance with the degree of dysfunction: with CC = 20-50 ml/min. - 125-250 mg 1-2 times/day, with CC = 10-19 ml/min. — 125 mg 1 time every 12-48 hours, with CC
Pharmacokinetics
When taken orally, it is absorbed from the gastrointestinal tract quickly and almost completely. Food intake has little effect on the speed and completeness of absorption. Bioavailability is 99%. Cmax is reached after 1-2 hours and when taking 250 mg and 500 mg it is 2.8 and 5.2 mcg/ml, respectively. Plasma protein binding is 30-40%. 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. Renal clearance accounts for 70% of the total clearance.
T1/2 - 6-8 hours. Excreted from the body mainly by the kidneys through glomerular filtration and tubular secretion. Less than 5% of levofloxacin is excreted as metabolites. Unchanged in urine, 70% is excreted within 24 hours and 87% within 48 hours; 4% of the dose taken orally is found in stool within 72 hours.
Indications for use Remedia 500 mg 10 pcs. film-coated tablets
Infections of the lower respiratory tract (chronic bronchitis, pneumonia), ENT organs (sinusitis, otitis media), urinary tract and kidneys (including acute pyelonephritis), genital organs (including urogenital chlamydia), skin and soft tissues (festering atheromas, abscess, boils).
Contraindications
Hypersensitivity, epilepsy, tendon damage due to previous treatment with quinolones, pregnancy, lactation, children and adolescents under 18 years of age.
Use levofloxacin with caution in elderly patients (high likelihood of concomitant decline in renal function).
Effect on the body
The drug has a wide spectrum of antimicrobial action.
Application of Remedia 500 mg 10 pcs. film-coated tablets during pregnancy and breastfeeding
Levofloxacin is contraindicated for use during pregnancy and lactation (breastfeeding).
Contraindicated in children and adolescents under 18 years of age.
special instructions
After normalization of the temperature, it is recommended to continue treatment for at least 48-78 hours. During treatment, it is necessary to avoid solar and artificial UV irradiation to avoid damage to the skin (photosensitization). If signs of tendonitis appear, levofloxacin is immediately discontinued. It should be borne in mind that in patients with a history of brain damage (stroke, severe trauma), seizures may develop; with glucose-6-phosphate dehydrogenase deficiency, there is a risk of hemolysis.
During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Overdose
Symptoms: nausea, erosive lesions of the gastrointestinal mucosa, prolongation of the QT interval, confusion, dizziness, convulsions.
Treatment: symptomatic.
Dialysis is ineffective. A specific antidote is not known.
Side effects of Remedia 500 mg 10 pcs. film-coated tablets
From the digestive system: nausea, vomiting, diarrhea, anorexia, abdominal pain, pseudomembranous enterocolitis, increased activity of liver transaminases, hyperbilirubinemia, hepatitis, dysbacteriosis.
From the cardiovascular system: decreased blood pressure, vascular collapse, tachycardia.
Metabolism: hypoglycemia (increased appetite, sweating, trembling).
From the central nervous system and peripheral nervous system: headache, dizziness, weakness, drowsiness, insomnia, paresthesia, anxiety, fear, hallucinations, confusion, depression, movement disorders, convulsions.
From the senses: disturbances of vision, hearing, smell, taste and tactile sensitivity.
From the musculoskeletal system: arthralgia, myalgia, tendon rupture, muscle weakness, tendonitis.
From the urinary system: hypercreatininemia, interstitial nephritis.
From the hematopoietic system: eosinophilia, hemolytic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhages.
Dermatological reactions: photosensitivity, itching, swelling of the skin and mucous membranes, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).
Allergic reactions: urticaria, bronchospasm, suffocation, anaphylactic shock, allergic pneumonitis, vasculitis.
Other: exacerbation of porphyria, rhabdomyolysis, persistent fever, development of superinfection.
Drug interactions
Increases the half-life of cyclosporine.
Drugs that inhibit intestinal motility, sucralfate, aluminum- and magnesium-containing antacid drugs, as well as drugs containing iron and zinc salts, reduce the effect of levofloxacin. The drug should be taken 2 hours before or 2 hours after taking these drugs.
Cimetidine and drugs that block tubular secretion slow down the elimination of levofloxacin.
Nonsteroidal anti-inflammatory drugs and theophylline increase the risk of seizures.
Glucocorticosteroids increase the risk of tendon rupture.
Hypoglycemic drugs increase the likelihood of hyper- and hypoglycemia, so strict control of blood glucose levels is necessary.
When used simultaneously with vitamin K antagonists, monitoring of blood clotting parameters is necessary.
Remedia film-coated tablets 500 mg 10 pcs
Hospital-acquired infections caused by Pseudomonas aeruginosa may require combination treatment.
The prevalence of acquired resistance in cultured strains of microorganisms may vary by geographic region and over time. Therefore, country-specific information on levofloxacin resistance 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.
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.
Like other quinolones, levofloxacin should be used with great caution in patients with a predisposition to seizures. These patients include patients with previous CNS lesions such as stroke, severe traumatic brain injury, patients concomitantly taking drugs that lower the seizure threshold of the brain, such as fenbufen and other similar NSAIDs or other drugs that lower the seizure threshold, such as theophylline.
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.
Tendonitis has been reported rarely with quinolones, including levofloxacin, and can sometimes 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 predisposed to developing tendonitis; in patients taking fluoroquinolones, the risk of tendon rupture may increase with simultaneous use of GCS. In addition, post-transplant patients have an increased risk of developing tendonitis, so it is recommended to be careful when prescribing fluoroquinolones to this category of patients. If tendonitis is suspected, treatment with levofloxacin should be stopped immediately and appropriate treatment of the affected tendon should be initiated, for example by providing adequate immobilization.
Levofloxacin may cause serious, potentially fatal hypersensitivity reactions (angioedema, anaphylactic shock), even with initial doses. In such cases, you should immediately stop using levofloxacin and consult a doctor.
Cases of severe bullous skin reactions such as Stevens-Johnson syndrome or toxic epidermal necrolysis have been observed with the use of levofloxacin. 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.
Cases of liver necrosis, including fatal liver failure, have been reported with the use of levofloxacin, mainly in patients with severe underlying diseases, such as sepsis. 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.
Since levofloxacin is excreted mainly through the kidneys, patients with impaired renal function require mandatory monitoring of renal function, as well as adjustment of the dosage regimen. When treating elderly patients, it should be taken into account that patients in this group often have impaired renal function.
Although photosensitivity occurs very rarely with the use of levofloxacin, to prevent its development, patients are not recommended to be exposed to strong solar or artificial ultraviolet radiation (for example, visiting a solarium) during treatment and for 48 hours after the end of treatment with levofloxacin.
As with the use of other antibiotics, the use of levofloxacin, especially for a long time, can lead to increased proliferation of microorganisms (bacteria and fungi) that are insensitive to it, which can cause changes in the microflora that is normally present in humans. As a result, superinfection may develop. Therefore, during treatment, it is imperative to re-evaluate the patient’s condition, and, if superinfection develops during treatment, appropriate measures should be taken.
Very rare cases of QT prolongation have been reported in patients taking fluoroquinolones, including levofloxacin.
When using fluoroquinolones, including levofloxacin, caution should be exercised in patients with known risk factors for prolongation of the QT interval: in patients with uncorrected electrolyte disturbances (with hypokalemia, hypomagnesemia), with congenital long QT syndrome, with heart disease (heart failure, myocardial infarction, bradycardia), with simultaneous use of drugs 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 in this category of patients.
Patients with latent or manifest glucose-6-phosphate dehydrogenase deficiency are predisposed to developing hemolytic reactions when treated with quinolones, which should be taken into account when treating with levofloxacin.
As with the use of other quinolones, cases of hyperglycemia and hypoglycemia have been observed with the use of levofloxacin. During therapy with levofloxacin, dysglycemia occurred more often in elderly patients and patients with diabetes mellitus receiving concomitant therapy with oral hypoglycemic drugs (for example, glibenclomide) or insulin. When using levofloxacin in such patients, the risk of developing hypoglycemia, including hypoglycemic coma, increases. It is necessary to inform patients about the symptoms of hypoglycemia (confusion, dizziness, ravenous appetite, headache, nervousness, palpitations or increased heart rate, pale skin, perspiration, trembling, weakness). If the patient develops hypoglycemia, treatment with levofloxacin should be stopped immediately and appropriate therapy should be initiated. In these cases, it is recommended to switch to therapy with an antibiotic other than a fluoroquinolone, if possible. When treating with levofloxacin in elderly patients and patients with diabetes mellitus, careful monitoring of blood glucose concentrations is recommended.
Sensory and sensorimotor peripheral neuropathy, which may have a rapid onset, has been reported in patients taking fluoroquinolones, including levofloxacin. If the patient develops symptoms of neuropathy, levofloxacin should be discontinued. This minimizes the possible risk of developing irreversible changes.
Fluoroquinolones, including levofloxacin, have neuromuscular blocking activity and may increase muscle weakness in patients with myasthenia gravis. 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.
The use of airborne anthrax is based on data on the sensitivity of Bacillus anthracis to it from in vitro and experimental studies in animals, as well as on 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, including suicidal ideation/attempts, have been reported in patients taking fluoroquinolones, including levofloxacin, sometimes after a single dose. In case of development of any side effects from the central nervous system, including mental disorders, treatment with levofloxacin should be stopped immediately and appropriate therapy should be prescribed. In these cases, it is recommended to switch to therapy with an antibiotic other than a fluoroquinolone, if possible. The drug should be prescribed with caution to patients with psychosis or patients with a history of mental illness.
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, which may subsequently lead to false-negative results of the bacteriological diagnosis of tuberculosis.
Remedia
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:
Microorganisms sensitive to levofloxacin (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.
