Levofloxacin (levofloxacinum) Euro solution for infusions 500 mg/100 ml. 100 ml.

Description

Levofloxacin Euro Storage:

active substance: levofloxacin;

100 ml of solution contains levofloxacin 500 mg (as levofloxacin hemihydrate);

Excipients: anhydrous glucose, edetate disodium, dilute hydrochloric acid, water for injections.

Dosage form. Solution for infusions.

Main physical and chemical properties: clear solution from yellow to greenish-yellow color, free from foreign particles.

Levofloxacin Euro Pharmacotherapeutic group.

Antibacterial agents of the quinolone group. Fluoroquinolones.

ATX code J01M A12.

Levofloxacin Euro Pharmacological properties.

Pharmacodynamics.

Levofloxacin is a synthetic antibacterial agent from the group of fluoroquinolones, the S (-) enantiomer of a racemic mixture of the drug ofloxacin.

Mechanism of action. Levofloxacin as an antibacterial drug from the group of fluoroquinolones acts on the complex of 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 genes
gyr-A.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.

Levofloxacin Euro Pharmacokinetics.

Absorption.

Levofloxacin is rapidly and almost completely absorbed when taken orally, with peak plasma concentrations reached within 1-2 hours. The absolute bioavailability is approximately 99-100%.

Food has almost no effect on the absorption of levofloxacin.

Steady state is reached within 48 hours at a dosage of 500 mg 1 or 2 times 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, epithelial lining fluid, alveolar macrophages, lung tissue, skin (blister content), prostate tissue and urine. However, levofloxacin is poorly absorbed into the cerebrospinal fluid.

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 is 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 is usually carried out by the kidneys (more than 85% of the administered dose). The mean pronounced total clearance of levofloxacin after administration of 1 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).