Levofloxacin solution for infusion 5mg/ml 100ml vial, 1pc – Dalkhimpharm

Composition

Pharmacological action

Broad-spectrum antimicrobial agent, fluoroquinolone. It acts bactericidal. It blocks DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and crosslinking 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. Food intake has little effect on the rate and completeness of absorption. Bioavailability is 99%. Cmax is reached after 1-2 hours and when taking 250 mg and 500 mg is 2.8 and 5.2 mcg / ml, respectively. Binding to plasma proteins is 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. Renal clearance is 70% of the total clearance. T1 / 2 – 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% is excreted in the urine within 24 hours and 87% in 48 hours; 4% of the oral dose is detected in the feces within 72 hours. After an intravenous infusion of 500 mg for 60 minutes, the Cmax is 6.2 mcg / ml. With intravenous single and multiple use, the apparent Vd after use of the same dose is 89-112 l, Cmax – 6.2 mcg/ml, T1/2 – 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), genitals (including urogenital chlamydia), skin and soft tissues (suppurated atheromas, abscess, boils).

Contraindications

Hypersensitivity, epilepsy, tendon damage during previous treatment with quinolones, pregnancy, lactation, children and adolescents under 18 years of age.

Side effects

From the digestive system: nausea, vomiting, diarrhea, anorexia, abdominal pain, pseudomembranous enterocolitis, increased activity of hepatic transaminases, hyperbilirubinemia, hepatitis, dysbiosis. From the cardiovascular system: reduced blood pressure, vascular collapse, tachycardia. From the side of 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, motor disorders, convulsions. From the side of the senses: visual, hearing, olfactory, taste and tactile sensitivity disorders. Musculoskeletal disorders: arthralgia, myalgia, tendon rupture, muscle weakness, tendinitis. From the urinary system: hypercreatininemia, interstitial nephritis. From the hematopoietic system: eosinophilia, hemolytic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhages. Dermatological reactions: photosensitivity, pruritus, edema 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. Others: exacerbation of porphyria, rhabdomyolysis, persistent fever, development of superinfection.

Interaction

Levofloxacin increases the T1 / 2 of cyclosporine. The effect of levofloxacin is reduced by drugs that inhibit intestinal motility, sucralfate, magnesium-and aluminum-containing antacids and iron salts (a break between use of at least 2 hours is necessary). Concomitant use of NSAIDs, theophylline increases convulsive readiness, and corticosteroids increase the risk of tendon rupture. Cimetidine and drugs that block tubular secretion slow down the elimination of levofloxacin. Levofloxacin solution for intravenous use 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). Levofloxacin solution for intravenous use should not be mixed with heparin and solutions that have an alkaline reaction.

How to take, course of use and dosage

Apply orally or intravenously. With sinusitis-inside,500 mg 1 time/day; with exacerbation of chronic bronchitis-250-500 mg 1 time/day. For pneumonia-inside,250-500 mg 1-2 times/day (500-1000 mg/day); iv-500 mg 1-2 times/day. For urinary tract infections-inside,250 mg 1 time/day or IV in the same dose. For skin and soft tissue infections-250-500 mg orally 1-2 times/day or iv,500 mg 2 times/day. After intravenous use in a few days, it is possible to switch to oral use at the same dose. In kidney diseases, the dose is reduced in accordance with the degree of impaired function: with creatinine clearance=20-50 ml / min-125-250 mg 1-2 times / day, with creatinine clearance=10-19 ml / min-125 mg 1 time in 12-48 hours, with creatinine clearance The duration of treatment is 7-10 (up to 14) days.

Special instructions

Levofloxacin is used with caution in elderly patients (there is a high probability of concomitant decrease in renal function). After normalization of temperature, it is recommended to continue treatment for at least 48-78 hours. The duration of an intravenous infusion of 500 mg (100 ml of infusioic solution) should be at least 60 minutes. During treatment, it is necessary to avoid sun and artificial UV radiation in order to avoid damage to the skin (photosensitization). If signs of tendinitis appear, levofloxacin is immediately discontinued. It should be borne in mind that patients with a history of brain damage (stroke, severe trauma) may develop seizures, and if glucose-6-phosphate dehydrogenase is insufficient, there is a risk of developing hemolysis. Influence on the ability to drive motor vehicles and control mechanisms During treatment, it is necessary to refrain from engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Active ingredient

Levofloxacin

Conditions of release from pharmacies

By prescription

Dosage form

solution for infusions

Description

Adults as prescribed by a doctor, Children as prescribed by a doctor, Children over 1 year of age

Indications

Bronchitis, From infectious diseases, From prostatitis, From urinary tract infections, From skin infections, From pneumonia, From sinusitis, From sinusitis, From tuberculosis, From respiratory tract infections, From boils, From inflammation of the female genital organs