Composition, form of production and packaging
The solution for infusions is transparent, greenish-yellow in color.
1 ml of 1 fl. (100 ml)
levofloxacin (in the form of hemihydrate) 500 mg 50 g
[PRING] sodium chloride 913.65 mg / 100 ml, disodium edetate 100 mg / 100 ml, hydrochloric acid 0.126 ml / 100 ml, sodium hydroxide 2.08 mg / 100 ml, water d / and up to 100 ml.
100 ml - plastic bottles (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Antimicrobial drug from the group of fluoroquinolones, the left-handed 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 gaps, inhibits DNA synthesis, causes profound morphological changes in the cytoplasm, cell wall and bacterial membranes. Levofloxacin is active against most strains of microorganisms both in vitro and in vivo.
In vitro sensitive (MPC <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-resistant methicillin-sensitive / moderately sensitive strains), Streptococcus spp. groups C and G (including Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus spp., viridans (penicillin-sensitive / resistant strains), aerobic gram-negative microorganisms: Acinetobacter baumannii , Acinetobacter spp., Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter aerobes, 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 catarrha lis (strains producing and non-producing beta-lactamase), Morganella morganii, Neisseria gonorrhoeae (strains producing and non-producing penicillinase), 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) for 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 thetaiotaomiСЃron, Bacteroides vulgatus, Bacteroides ovatus, Prevotella spp., Porphyromonas spp.
To levofoloxacin resistant (MIC> 8 mg / h) aerobic Gram-positive microorganisms: 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
Binding to proteins - 30-40%. Cumulation at a dose of 500 mg 1 time / day is insignificant. When administered at a dose of 500 mg 2 times / day, cumulation can be observed to a small extent. C ss are achieved 3 days after the start of the application.
It penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, urinary system organs, genital organs, bone tissue, prostate gland, polymorphonuclear leukocytes, alveolar macrophages. Levofloxacin poorly penetrates into the cerebrospinal fluid.
Average concentrations in the urine 8-12 hours after a single administration 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 undergoes metabolism with the formation of desmethyllevofloxacin and levofloxacin-N-oxide, which constitute <5% of the levofloxacin output by the kidneys.
Excretion
After the administration of a single dose of 500 mg of T 1/2 is 6-8 hours. It is excreted mainly by the kidneys through glomerular filtration and tubular secretion. Less than 5% of levofloxacin is excreted as metabolites. In unchanged form, 70% are deduced and 87% for 48 hours.
INDICATIONS
Infectious-inflammatory diseases caused by microorganisms sensitive to levofloxacin;
- infections of the lower respiratory tract (exacerbation of chronic bronchitis, community-acquired pneumonia);
acute acute maxillary sinusitis;
uncomplicated urinary tract infections;
- Complicated urinary tract infections (including acute pyelonephritis):
- skin and soft tissue infections (festering atheromas, abscess, boils);
- septicemia / bacteremia;
- chronic bacterial prostatitis;
- intra-abdominal infection;
- complex therapy of drug-resistant forms of tuberculosis.
DOSING MODE
The drug is injected / drip. The duration of IV infusion of 500 mg of levofloxacin (100 ml of infusion solution) should be at least 60 minutes. Doses are determined by the nature and severity of the infection, as well as the suspected pathogen susceptibility.
Patients with normal renal function (creatinine clearance> 50 ml / min) are recommended the following dosing regimen:
- exacerbation of chronic bronchitis: 250-500 mg of levofloxacin 1 time / day for 7-10 days;
- community-acquired pneumonia : 500 mg of levofloxacin 1-2 times / day for 7-14 days;
- acute maxillary sinusitis: 500 mg of levofloxacin once a day for 10-14 days;
- uncomplicated urinary tract infections: 250 mg of levofloxacin 1 time / day for 3 days;
- Complicated urinary tract infections (including acute pyelonephritis): 250 mg of levofloxacin 1 time / day for 7-10 days;
- skin and soft tissue infections: 500 mg of levofloxacin 2 times / day for 7-14 days;
- septicemia / bacteremia : 500 mg of levofloxacin 1-2 times / day for 10-14 days;
- chronic bacterial prostatitis: 500 mg of levofloxacin 1 time / day for 28 days;
- intra-abdominal infection: 500 mg of levofloxacin 1 time / day for 7-14 days (in combination with antibacterial drugs acting on anaerobic flora);
- complex therapy of drug-resistant forms of tuberculosis: 500 mg of levofloxacin 1-2 times / day until 3 months.
Patients with impaired renal function (creatinine clearance <50 mL / min) are recommended the following dosing regimen:
Creatinine clearance (ml / min) Dose for intravenous administration
250 mg / 24 h 500 mg / 24 h 500 mg 12 h
Initial dose Initial dose Initial dose
250 mg 500 mg 500 mg
50-20 Further 125 mg / 24 hours Further 250 mg / 24 hours Further 250 mi 12 hours
<19-10 Further 125 mg / 48 h Further 125 mg / 24 h Further 125 mg / 12 h
<10 (including hemodialysis and permanent ambulatory peritoneal dialysis) Further 125 mg / 48 h Further 125 mg / 24 h Further 125 mg / 24 h
After hemodialysis or continuous outpatient peritoneal dialysis (PDLP), no additional doses are required.
If the liver function is not corrected, dose adjustment is not required, because Levofloxacin is metabolized in the liver to an insignificant degree.
Depending on the patient's condition after a few days of treatment, you can go from / in the drip to receive the same dose of the drug in a form intended for oral administration.
SIDE EFFECT
On the part of the digestive system: nausea, vomiting, diarrhea (including with blood), digestive disorders, decreased appetite, abdominal pain, pseudomembranous colitis, increased activity of hepatic transaminases, hyperbilirubinemia, hepatitis, dysbiosis.
From the cardiovascular system: a decrease in blood pressure, vascular collapse, tachycardia, an increase in the QT interval on a cardiogram, atrial fibrillation.
On the part of metabolism: hypoglycemia (increased appetite, increased sweating, trembling, nervousness), hyperglycemia.
From the side of the nervous system: headache, dizziness, weakness, drowsiness, insomnia, anxiety, paresthesia in the hands, fear, hallucinations, confusion, depression, motor disorders, seizures, peripheral sensory neuropathy, peripheral sensory-motor neuropathy, mental disorders with violations of behavior with self-harm, including suicidal thoughts and suicidal attempts.
From the senses: visual, hearing, smell, taste and tactile sensitivity.
From the musculoskeletal system: arthralgia, muscle weakness, myalgia, tendon rupture, tendonitis, rhabdomyolysis.
From the side of the urinary system: hypercreatininaemia, interstitial nephritis, acute renal failure.
On the part of the organs of hematopoiesis: eosinophilia, hemolytic anemia, leukopenia, neutropenia, agranulocytosis. thrombocytopenia, pancytopenia, hemorrhage.
Allergic reactions: itching and hyperemia of the skin, swelling of the skin and mucous membranes, urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), bronchospasm, anaphylactic shock, allergic pneumonitis, vasculitis.
Other: asthenia, exacerbation of porphyria, photosensitivity, persistent fever, leukocytoclastic vasculitis, development of superinfection.
Local reactions: pain, redness at the injection site, phlebitis.
CONTRAINDICATIONS
- epilepsy;
- damage to the tendons during the previous treatment with quinolones;
- Pregnancy;
- lactation period;
- Children and adolescence (up to 18 years);
- hypersensitivity to levofloxacin, any other component of the drug, or other drugs from the group of fluoroquinolones.
Precautions: elderly age (high probability of concomitant decrease in kidney function), deficiency of glucose-6-phosphate dehydrogenase, in patients with a history of brain injury (stroke or severe trauma), in patients simultaneously receiving drugs lowering the threshold of convulsive readiness of the brain (possible convulsions), in patients with pseudo-paralytic myasthenia gravis (myasthenia grais), with known risk factors for prolonging the QT interval.
PREGNANCY AND LACTATION
The drug is contraindicated in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with impaired renal function (creatinine clearance <50 mL / min) are recommended the following dosing regimen:
Creatinine clearance (ml / min) Dose for intravenous administration
250 mg / 24 h 500 mg / 24 h 500 mg 12 h
Initial dose Initial dose Initial dose
250 mg 500 mg 500 mg
50-20 Further 125 mg / 24 hours Further 250 mg / 24 hours Further 250 mi 12 hours
<19-10 Further 125 mg / 48 h Further 125 mg / 24 h Further 125 mg / 12 h
<10 (including hemodialysis and permanent ambulatory peritoneal dialysis) Further 125 mg / 48 h Further 125 mg / 24 h Further 125 mg / 24 h
After hemodialysis or continuous outpatient peritoneal dialysis (PDLP), no additional doses are required.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
If the liver function is not corrected, dose adjustment is not required, because Levofloxacin is metabolized in the liver to an insignificant degree.
APPLICATION FOR CHILDREN
Contraindicated in children under the age of 18 years.
APPLICATION IN ELDERLY PATIENTS
With caution: elderly age (high probability of concomitant decrease in kidney function).
SPECIAL INSTRUCTIONS
When the body temperature is normal, it is recommended to continue treatment for at least 48-72 hours.
During treatment it is necessary to avoid sunlight and artificial ultraviolet irradiation to avoid damage to the skin (photosensitization). When there are signs of tendinitis, pseudomembranous colitis, allergic reactions, levofloxacin is immediately canceled.
It should be borne in mind that the development of seizures is possible in patients with a history of brain injury (stroke or severe trauma), while the risk of hemolysis of erythrocytes is insufficiency of glucose-6-phosphate dehydrogenase.
During treatment, alcohol should be avoided.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, care must be taken when driving and potentially dangerous mechanisms due to possible dizziness, drowsiness, stiffness and visual disturbances, which can lead to a slowing of the speed of psychomotor reactions and a decrease in the ability to concentrate.
OVERDOSE
Symptoms: manifested mainly from the side of the central nervous system (confusion, dizziness, impaired consciousness and convulsions as epileptic seizures).
In addition, gastrointestinal disorders (eg, nausea) and erosive lesions of the gastrointestinal mucous membranes, prolongation of the QT interval can be noted.
Treatment: symptomatic. Dialysis is ineffective. The specific antidote is not known.
DRUG INTERACTION
Levofloxation increases T 1/2 cyclosporin.
NSAIDs, theophylline increase the risk of developing seizures.
Acceptance of GCS increases the risk of rupture of tendons (especially in old age).
Cimetidine and drugs that block tubular secretion, slow the withdrawal of levofloxacin.
Solution for infusion 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).
Do not mix with heparin and solutions that have an alkaline reaction (for example, with sodium bicarbonate solution).
In patients with diabetes mellitus receiving oral hypoglycemic agents or insulin, against the background of the administration of levofloxacin hypo- and hyperglycemic conditions are possible, therefore it is recommended to control the concentration of glucose in the blood.
Levofloxacin increases the anticoagulant activity of warfarin
Alcohol can increase the side effects of the central nervous system (dizziness, numbness, drowsiness).
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
Store in a dry, dark place at a temperature of no higher than 25 В° C. Do not freeze.
Keep out of the reach of children.
Shelf life - 2 years. Do not use after expiry date.
