Levoximed solution for infusions 500 mg/100 ml. 100 ml. vial №1

Description

Levoximed Storage
active substance: levofloxacin;

100 ml of solution contains levofloxacin (in the form of levofloxacin hemihydrate) 500 mg;

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

Levoximed Dosage form
Solution for infusion.

Main physical and chemical properties: clear solution of greenish-yellow color.

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

Levoximed Pharmacological properties
Pharmacodynamics.

Levofloxacin – a synthetic antibacterial agent from the group of fluoroquinolones,

S-enantiomer of a racemic mixture of ofloxacin.

Mechanism of action

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 plasma concentration (Cmax) or the area under the pharmacokinetic curve (AUC) and the minimum inhibitory (inhibitory) concentration (MIC).

Mechanism of resistance

Resistance to levofloxacin develops as a stepwise mutation of the target site in both types of topoisomerase II, DNA gyrase and topoisomerase IV. Other mechanisms of resistance, such as permeability (characteristic of Pseudomonas aeruginosa) and outflow mechanisms, may also affect sensitivity to levofloxacin.

There is cross-resistance between levofloxacin and other fluoroquinolones. Due to the mechanism of action, there is no cross-resistance between levofloxacin and other classes of antibacterial agents.

Limit values

The MIC limit values ​​for levofloxacin recommended by the European Committee for Antimicrobial Susceptibility Testing (EUCAST), which separate susceptible micro-organisms from intermediate-susceptible (moderately resistant) and intermediate-sensitive from resistant organisms, are presented in the table below.

Absorption

There is no significant difference in the pharmacokinetics of levofloxacin after intravenous and oral administration.

Distribution

Following intravenous administration, approximately 30–40% of levofloxacin is bound to plasma protein. The mean volume of distribution of levofloxacin is about 100 l after a single and repeated dose of 500 mg, indicating good distribution in body tissues.

Penetration into tissues and body fluids

Levofloxacin has been shown to penetrate the bronchial mucosa, bronchoalveolar fluid, alveolar macrophages, lung tissue, skin (blister), prostate tissue and urine. It penetrates poorly into the cerebrospinal fluid.

Metabolism

Levofloxacin is metabolized to a very small extent, the metabolites being dimethyl-levofloxacin and levofloxacin N-oxide. These metabolites make up less than 5% of the amount of the parent compound excreted in the urine. Levofloxacin is stereochemically stable and is not subject to inversion of the choral structure.