Assign to adults for the treatment of infections caused by microorganisms sensitive to the drug: community-acquired pneumonia; complicated skin and soft tissue infections; (For the above-mentioned infections, Levofloxacin should only be used when the use of other antibacterial agents that are usually recommended for the initial treatment of these infections is impractical or impossible); pyelonephritis, complicated urinary tract infections; chronic bacterial prostatitis.
Levofloxacin solution infusions Storage
active substance: levofloxacin;
100 ml of solution contains levofloxacin hemihydrate in terms of anhydrous 100% levofloxacin 500 mg;
Excipients: sodium chloride, disodium edetate, dilute hydrochloric acid, sodium hydroxide, water for injections.
Levofloxacin solution Dosage form
Solution for infusion.
Main physical and chemical properties: clear liquid from yellow to greenish-yellow color. Theoretical osmolarity – 300 mosmol / l.
Levofloxacin solution Pharmacotherapeutic group
Antibacterial agents of the quinolone group. Fluoroquinolones.
ATX code J01M A12.
Levofloxacin solution Pharmacological properties
Levofloxacin is a synthetic antibacterial agent from the group of fluoroquinolones, S ‑ enantiomer of a racemic mixture of the drug ofloxacin.
Mechanism of action
As an antibacterial drug from the group of fluoroquinolones, levofloxacin acts on the complex of DNA-DNA gyrase and topoisomerase IV.
Pharmacokinetic / pharmacodynamic ratio
The degree of bacterial activity of levofloxacin depends on the ratio of the maximum serum concentration (Cmax) or the area under the pharmacokinetic curve (AUC) and the minimum inhibitory (inhibitory) concentration (MIC).
Mechanism of resistance
The main mechanism of resistance is due to mutations in gyr-A genes. In vitro, there is cross-resistance between levofloxacin and other fluoroquinolones.
Due to the mechanism of action, there is usually no cross-resistance between levofloxacin and other classes of antibacterial agents.
There is no significant difference between the pharmacokinetics of levofloxacin after intravenous and oral administration.
Steady state is reached within 48 hours at a dosage of 500 mg once or twice a day.
Approximately 30-40% of levofloxacin is bound to serum protein. The mean volume of distribution of levofloxacin is about 100 l after a single and repeated dose of 500 mg, indicating its widespread distribution in body tissues.
Penetration into tissues and body fluids
Levofloxacin has the ability to penetrate the bronchial mucosa, alveolar epithelial fluid, alveolar macrophages, lung tissue, skin (blister content), prostate tissue and urine. However, levofloxacin does not penetrate the cerebrospinal fluid well.
Levofloxacin is metabolized to a very small extent, the metabolites being dimethyl-levofloxacin and levofloxacin N-oxide. These metabolites account for less than 5% of the drug excreted in the urine. Levofloxacin is stereochemically stable and not subject to inversion of the chiral structure.
After oral and intravenous administration, levofloxacin is excreted from the blood plasma relatively slowly (half-life is 6-8 hours). Excretion usually occurs by the kidneys (more than 85% of the administered dose). The mean pronounced total clearance of levofloxacin after a single dose of 500 mg was 175 ± 29.2 ml / min. There is no significant difference in the pharmacokinetics of levofloxacin after intravenous and oral administration, indicating the interchangeability of these pathways (oral and intravenous).