Levinor solution for infusions 0.5% 100 ml.

Description

Levinor Storage
active substance: levofloxacin;

100 ml of solution contain levofloxacin hemihydrate in terms of anhydrous 100% levofloxacin 500 mg;

Excipients: sodium chloride, disodium edetate, dilute hydrochloric acid, sodium hydroxide, water for injections.

Levinor Dosage form
Solution for infusion.

Main physical and chemical properties: clear liquid from yellow to greenish-yellow color. Theoretical osmolarity – 300 mosmol / l.

Levinor Pharmacotherapeutic group
Antibacterial agents of the quinolone group. Fluoroquinolones. ATX code J01M A12.

Pharmacological properties
Pharmacodynamics.

Levofloxacin is a synthetic antibacterial agent from the class of fluoroquinolones, S ‑ enantiomer of a racemic mixture of the drug ofloxacin.

Levinor Mechanism of action.

As an antibacterial drug of the fluoroquinolone class, levofloxacin acts on the complex of DNA-DNA gyrase and topoisomerase IV.

The ratio of pharmacokinetics (FC) / pharmacodynamics (PD).

The degree of bactericidal 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 concentration (MIC).

Mechanism of resistance.

Resistance to levofloxacin develops gradually due to mutations in the target genes of topoisomerase type II, DNA gyrase and topoisomerase IV. Other mechanisms of resistance, such as decreased bacterial permeability (Pseudomonas aeruginosa) and efflux mechanisms, may affect susceptibility to levofloxacin. 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.

Absorption.

Orally administered levofloxacin is rapidly and almost completely absorbed, reaching peak plasma concentrations within 1-2 hours. The absolute bioavailability is 99–100%. Food has little effect on the absorption of levofloxacin.

Steady state is reached within 48 hours at a dosage of 500 mg once or twice a day.

Distribution.

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.

Biotransformation.

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.

Breeding.

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).