Levomak 750 coated tablets 750 mg. №10

Description

Levomak Storage:

active substance: levofloxacin;

1 tablet contains levofloxacin hemihydrate equivalent to levofloxacin 750 mg;

Excipients: microcrystalline cellulose, crospovidone, hypromellose, magnesium stearate, titanium dioxide (E 171), polyethylene glycol 400, polysorbate 80, iron oxide red (E 172), iron oxide yellow (E 172).

Levomak Dosage form. Film-coated tablets.

Main physical and chemical properties: biconvex oblong tablets, film-coated brown-red, with notches T and 64 and the fracture line on one side and the fracture line on the other side.

Levomak Pharmacotherapeutic group.

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

Levomak Pharmacological properties.

Pharmacodynamics.

Levofloxacin is a synthetic antibacterial agent of the fluoroquinolone group, the S-enantiomer of a racemic mixture of the drug ofloxacin.

Mechanism of action.

As an antibacterial drug of the fluoroquinolone group, 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 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 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.

Absorption

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

Food has almost no effect on the absorption of levofloxacin.

Distribution

Approximately 30-40% of levofloxacin is bound to serum protein. The cumulative effect of repeated administration of levofloxacin with the use of 500 mg 1 time per day is almost absent. There is a small but predictable cumulative effect after taking a dose 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 lung secretion after oral administration of 500 mg was 8.3 μg / g and 10.8 μg / ml, respectively. These values ​​were achieved within 1 hour after taking the drug.

Penetration into lung tissue

Peak concentrations of levofloxacin in lung tissue after oral administration of 500 mg were approximately 11.3 μg / g and were reached 4-6 hours after administration. The concentration in the lungs exceeds that in blood plasma.

Penetration into the contents of the bladder

Maximum concentrations of levofloxacin 4-6.7 μg / ml in the contents of the bladder were reached in 2-4 hours after taking the drug after 3 days of taking the drug at a dose of 500 mg 1-2 times a day, respectively.