Levomak solution for infusions 500 mg/100 ml. 100 ml. №1

Description

Levomak solution  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.

Levomak solution  Dosage form
Solution for infusion.

Main physical and chemical properties: clear liquid from yellow to greenish-yellow color.

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

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. As an antibacterial drug from the group of fluoroquinolones, levofloxacin acts on the complex of DNA-DNA gyrase and topoisomerase IV.

Pharmacokinetic / pharmacodynamic ratioThe degree of bacterial activity of levofloxacin depends on the ratio of the maximum serum concentration (Cmax) or the area under the pharmacokinetic curve “concentration-time” (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.

Other data. Nosocomial infections caused by P. aeruginosa may require combination therapy.

Pharmacokinetics.

Levomak solution  Absorption

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

After intravenous administration, the drug accumulates in the bronchial mucosa and bronchial secretions of lung tissue (concentration in the lungs exceeds that in blood plasma), urine. Levofloxacin enters the cerebrospinal fluid poorly.

Distribution

Approximately 30–40% of levofloxacin is bound to serum protein. The cumulative effect of levofloxacin when using 500 mg 1 time per day with repeated use is almost absent. There is a small but predictable cumulative effect after administration of doses of 500 mg 2 times a day. Stable state is reached within 3 days.

Penetration into tissues and body fluids

Penetration into the bronchial mucosa, bronchial secretion of lung tissue (BSTL)

The maximum concentration of levofloxacin in the bronchial mucosa and bronchial secretions after administration of 500 mg orally was 8.3 μg / g and 10.8 μg / ml, respectively. These values ​​were achieved within one hour after taking the drug.

Penetration into lung tissue

The maximum concentration of levofloxacin in lung tissues after administration of 500 mg orally was approximately 11.3 μg / g and was reached 4-6 hours after administration of the drug. The concentration in the lungs exceeds that in blood plasma.

Penetration into the contents of the pustule

The maximum concentration of levofloxacin 4–6.7 μg / ml in the contents of the pustule was reached in 2–4 hours after drug administration after 3 days of drug use at doses of 500 mg 1 or 2 times a day, respectively.

Penetration into the cerebrospinal fluid

Levofloxacin does not penetrate well into the cerebrospinal fluid.

Penetration into prostate tissue

After administration of 500 mg of levofloxacin once a day for 3 days, the average concentration in prostate tissue reached 8.7 μg / g, 8.2 μg / g and 2 μg / g, respectively, after 2 hours, 6 hours and 24 hours; the average prostate / plasma concentration ratio was 1.84.

Concentration in urine

The mean urinary concentration 8–12 hours after a single oral dose of 150 mg, 300 mg, or 500 mg levofloxacin was 44 mg / L, 91 mg / L, or 200 mg / L, respectively.

Biotransformation

Levofloxacin is slightly metabolized, 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).

There is no significant difference in the pharmacokinetics of levofloxacin after intravenous and oral administration, indicating that these pathways (oral and intravenous) are interchangeable.