Levofloxacin-Novofarm solution for infusions 5 mg/ml. 100 ml. №1

Description

Levofloxacin-Novofarm Storage

active substance: levofloxacin hemihydrate;

1 ml of solution contains levofloxacin hemihydrate in terms of levofloxacin 5 mg;

Excipients: sodium chloride, sodium hydroxide, concentrated hydrochloric acid, water for injections.

Levofloxacin-Novofarm Dosage form

Solution for infusion.

Main physical and chemical properties: clear solution of greenish-yellow color. Theoretical osmolarity – 302 mosmol / l.

Pharmacotherapeutic group. Antibacterial agents of the quinolone group. Fluoroquinolones.

ATX code J01M A12.

Levofloxacin-Novofarm 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-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).

Levofloxacin-Novofarm 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.

Checkpoints

The European Antimicrobial Susceptibility Testing Committee (EUCAST) recommended levofloxacin MIC limit values ​​separating susceptible micro-organisms from intermediate-susceptible (moderately resistant) and intermediate-susceptible from resistant organisms are presented in Table 1 of the test.

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 a single dose of 500 mg was 175 ± 29.2 ml / min. There is no significant difference in the pharmacokinetics of levofloxacin after oral and intravenous administration, indicating the interchangeability of these pathways (oral and intravenous).