Description
Pharmacological action
Broad-spectrum antimicrobial agent, fluoroquinolone. It is bactericidal. It blocks DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA breaks, inhibits DNA synthesis, and causes deep 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.
Pharmacokinetics
When taken orally, it is absorbed from the gastrointestinal tract quickly and almost completely. Eating little effect on the speed and completeness of absorption. Bioavailability is 99%. Cmax is reached after 1-2 hours and when taken with 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, mucous membrane of the bronchi, sputum, organs of the genitourinary system, polymorphonuclear leukocytes, alveolar macrophages. In the liver, a small portion is oxidized and / or deacetylated. Renal clearance is 70% of the total clearance.
T1 / 2 – 6-8 hours. It is excreted mainly by the kidneys by glomerular filtration and tubular secretion. Less than 5% of levofloxacin is excreted as metabolites. In unchanged form, with urine within 24 hours, 70% is excreted and in 48 hours – 87% in feces for 72 hours, 4% of the oral dose is found. After iv infusion of 500 mg for 60 min Cmax – 6.2 Ојg / ml. With iv single and multiple administration, the apparent Vd after administration of the same dose is 89-112 L, Cmax – 6.2 Ојg / ml, T1 / 2 – 6.4 hours
Indications
Lower respiratory tract infections (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 atheroma, abscess, boils).
Contraindications
Hypersensitivity, epilepsy, tendon damage with previous treatment with quinolones, pregnancy, lactation, children and adolescents under 18 years of age.
Special instructions
Levofloxacin is used with caution in elderly patients (there is a high likelihood of a concomitant decrease in renal function).
After normalizing the temperature, it is recommended to continue treatment for at least 48-78 hours. The duration of iv infusion of 500 mg (100 ml of infusion solution) should be at least 60 minutes. During treatment, it is necessary to avoid solar and artificial UV radiation in order to avoid damage to the skin (photosensitivity). When signs of tendonitis appear, levofloxacin is immediately canceled. 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.
Influence on the ability to drive vehicles and control mechanisms
During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities, requiring increased concentration of attention and speed of psychomotor reactions.
Composition
Infusion solution 1 ml
levofloxacin 5 mg
Dosage and administration
Used orally or iv.
In case of 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) IV – 500 mg 1-2 times / day. In case of urinary tract infections, by mouth, 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 administration, after a few days, it is possible to switch to oral administration in the same dose.
In case of kidney disease, the dose is reduced in accordance with the degree of dysfunction: with KK = 20-50 ml / min – 125-250 mg 1-2 times / day, with KK = 10-19 ml / min – 125 mg 1 time per 12-48 hours, with CC <10 ml / min - 125 mg after 24 or 48 hours. The duration of treatment is 7-10 (up to 14) days. Side effects of the Digestive system: nausea, vomiting, diarrhea, anorexia, abdominal pain, pseudomembranous enterocolitis, increased activity of hepatic transaminases, hyperbilirubinemia, hepatitis, dysbiosis. From the cardiovascular system: decreased blood pressure, vascular collapse, tachycardia. From the side of 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, motor disorders, cramps. On the part of the sensory organs: impaired 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 hemopoietic system: eosinophilia, hemolytic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhage. 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. active substance Levofloxacin Terms of delivery from pharmacies Prescription Dosage form infusion solution Indications From prostatitis, From tuberculosis, From hyperplasia, prostate7 AT tons of boils, from skin infections, from respiratory tract infections, from pneumonia, from urinary tract infections, from inflammation of the female genital organs, from tuberculosis, from sinusitis, from sinusitis, from infectious diseases, From prostatitis, bronchitis