Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antimicrobial agent of a wide spectrum of action, fluoroquinolone. It is bactericidal. It 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 membranes.
It is 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.
PHARMACOKINETICS
When taken orally absorbed from the gastrointestinal tract quickly and almost completely. Food intake has little effect on the speed and completeness of absorption.Bioavailability is 99%. C max is achieved in 1-2 hours and when taking 250 mg and 500 mg is 2.8 and 5.2 Ојg / ml, respectively. Binding to plasma proteins - 30-40%. It penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, organs of the genitourinary system, polymorphonuclear leukocytes, alveolar macrophages.In the liver, a small portion is oxidized and / or deacetylated. Kidney clearance is 70% of the total clearance.
T 1/2 - 6-8 hours. Excreted mainly by the kidneys through glomerular filtration and tubular secretion. Less than 5% of levofloxacin is excreted as metabolites. In unchanged form with urine within 24 hours 70% are deduced and in 48 hours - 87%; in the stool for 72 hours 4% of the dose taken internally is detected. After intravenous infusion of 500 mg for 60 min C max - 6.2 Ојg / ml. With IV single and multiple administration, the apparent V d after administration of the same dose is 89-112 L, C max is 6.2 Ојg / ml, T 1/2 is 6.4 h.
INDICATIONS
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).
DOSING MODE
Applied inside or / in.
With sinusitis - inside, 500 mg 1 time / day; with exacerbation of chronic bronchitis - 250-500 mg 1 time / day. With pneumonia - inside, 250-500 mg 1-2 times / day (500-1000 mg / day); in / in - 500 mg 1-2 times / day. With infections of the urinary tract - inside, 250 mg 1 time / day or IV in the same dose. With infections of the skin and soft tissues - 250-500 mg orally 1-2 times / day or IV, 500 mg 2 times / day. After iv introduction in a few days, you can switch to oral administration at the same dose.
In case of kidney diseases, the dose is reduced in accordance with the degree of disruption of the function: with KK = 20-50 ml / min - 125-250 mg 1-2 times / day, with KK = 10-19 ml / min - 125 mg once every 12 -48 h, with CC <10 ml / min - 125 mg after 24 or 48 hours. The duration of treatment is 7-10 (up to 14) days.
SIDE EFFECT
On the part of the digestive system: nausea, vomiting, diarrhea, anorexia, abdominal pain, pseudomembranous enterocolitis, increased activity of hepatic transaminases, hyperbilirubinemia, hepatitis, dysbiosis.
From the cardiovascular system: a decrease in blood pressure, vascular collapse, tachycardia.
From the metabolism: hypoglycemia (increased appetite, sweating, trembling).
From the side of 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: visual, hearing, smell, taste and tactile sensitivity.
From the musculoskeletal system: arthralgia, myalgia, rupture of tendons, muscle weakness, tendonitis.
From the side of the urinary system: hypercreatininaemia, interstitial nephritis.
From the hemopoietic system: eosinophilia, hemolytic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhages.
Dermatological reactions: photosensitization, itching, swelling of the skin and mucous membranes, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).
Allergic reactions: urticaria, bronchospasm, choking, anaphylactic shock, allergic pneumonitis, vasculitis.
Other: exacerbation of porphyria, rhabdomyolysis, persistent fever, development of superinfection.
CONTRAINDICATIONS
Hypersensitivity, epilepsy, tendon damage with previously treated quinolones, pregnancy, lactation, children and adolescence under 18 years.
PREGNANCY AND LACTATION
Levofloxacin is contraindicated in pregnancy and lactation (breastfeeding).
APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 18 years.
APPLICATION IN ELDERLY PATIENTS
With caution appoint levofloxacin to elderly patients (high probability of concomitant decrease in kidney function).
SPECIAL INSTRUCTIONS
With caution use levofloxacin in elderly patients (high probability of concomitant decrease in kidney function).
After normalizing the temperature, it is recommended to continue treatment at least 48-78 hours. The duration of IV infusion of 500 mg (100 ml infusion solution) should be at least 60 minutes. During treatment, sun and artificial UV irradiation should be avoided to avoid damage to the skin (photosensitivity). When there are signs of tendonitis, levofloxacin is immediately withdrawn. It should be borne in mind that the development of seizures is possible in patients with a history of brain injury (stroke, severe trauma), with the insufficiency of glucose-6-phosphate dehydrogenase - the risk of hemolysis.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.
DRUG INTERACTION
Levofloxacin increases T 1/2 cyclosporin.
The effect of levofloxacin reduces drugs that depress intestinal motility, sucralfate, magnesium and aluminum-containing antacids and iron salts (a break between intake of at least 2 hours is necessary).
With the simultaneous use of NSAIDs, theophylline increases convulsive readiness, GCS - increase the risk of rupture of tendons.
Cimetidine and drugs that block tubular secretion, slow the withdrawal of levofloxacin.
A solution of levofloxacin for IV administration is compatible with 0.9% sodium chloride solution, 5% dextrose solution, 2.5% Ringer's dextrose solution, combined solutions for parenteral nutrition (amino acids, carbohydrates, electrolytes).
A solution of levofloxacin for intravenous administration should not be mixed with heparin and solutions that have an alkaline reaction.
