Levostad coated tablets 500 mg. №5

Description

Levostad  Storage
active substance: levofloxacin;

1 film-coated tablet contains 250 mg or 500 mg of levofloxacin (as levofloxacin hemihydrate);

excipients: microcrystalline cellulose; cellulose powder; pregelatinized starch; corn starch; crospovidone; povidone; hypromellose; sodium stearyl fumarate; polyethylene glycol; lactose monohydrate; titanium dioxide (E 171); iron oxide red (E 172); iron oxide yellow (E 172); iron oxide black (E 172).

Levostad  Dosage form
Film-coated tablets.

Basic physical and chemical properties: pink tablets, film-coated, oval, with a line on both sides.

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, is the S (-) enantiomer of a racemic mixture of the drug ofloxacin.

The bactericidal effect is provided due to the inhibition by levofloxacin of the bacterial enzyme DNA gyrase, which belongs to type II topoisomerases. The result of such suppression is the impossibility of the transition of bacterial DNA from a state of relaxation to an over-twisted state, which, in turn, makes it impossible for further division (reproduction) of bacterial cells. The spectrum of activity of levofloxacin includes gram-positive and gram-negative bacteria together with non-fermenting bacteria.

Microorganisms sensitive to the drug:

Gram-positive aerobes: Enterococcus faecalis (moderately sensitive), Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus saprophyticus, Streptococci, group C and G, Streptococcus agalactiae, Streptococcus pneumoniae (including penicillin).

Gram-negative aerobes: Burkholderia cepacia, Eikenella corrodens, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis, Pasteurella multocida, Proteus vulgaris, Providencia rettgeri.

Anaerobes: Peptostreptococcus.

Others: Chlamydia pneumoniae, Mycoplasma pneumoniae, Chlamydia psitacci, Chlamydia trachomatis, Legionella pneumophila, Mycoplasma hominis, Ureaplasma urealyticum.

Microorganisms to which sensitivity may develop.

Gram-positive aerobes: Enterococcus faecalis, Staphylococcus aureus (methicillin-resistant strains), Coagulase negative Staphylococcus spp.

Gram-negative aerobes: Escherichia coli, Enterobacter cloacae, Salmonella species, Proteus mirabilis, Pseudomonas aeruginosa, Acinetobacter baumanii, Citrobacter freundii, Enterobacter aerogenes, Enterobacter agglomerans, Morganella morganici, Providenciarati.

Anaerobic bacteria: Bacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus, Clostridium difficile.

Levostad  Pharmacokinetics.

Absorption

Orally administered levofloxacin is rapidly and almost completely absorbed; the peak of concentration in blood plasma is observed in 1-2 hours after reception. Absolute bioavailability – almost 100%. Eating has some effect on its absorption.

Levostad Distribution

Approximately 30-40% of levofloxacin is bound to serum protein. The cumulative effect of levofloxacin at a dosage of 500 mg 1 time per day has no clinical significance and can be neglected. There is a small but expected accumulation at a dosage of 500 mg 2 times a day. Stabilization is achieved after 3 days of use.

Penetration into tissues and body fluids.

Penetration into bronchial mucus, epithelial serous fluid

The maximum concentration of levofloxacin in bronchial mucus, bronchoalveolar lavage fluid after administration of 500 mg is 8.2 mg / g and 10.8 mg / g and is reached 1 hour after application.

Penetration into the lung tissue

The maximum concentration of levofloxacin in lung tissue after application of 500 mg is approximately 11.3 mg / g and is reached in 4-6 hours after application. The concentration of levofloxacin in lung tissue significantly exceeds its concentration in blood plasma.

Penetration into the contents of the blister

The maximum concentration of levofloxacin in the contents of the blister after application of 500 mg 1-2 times a day for 3 days is approximately 4.0-6.7 mg / g and is reached in 2-4 hours after application.

Penetration into the cerebrospinal fluid

Almost does not penetrate.

Penetration into prostate tissue

The mean concentration of levofloxacin in prostate tissue after administration of 500 mg once daily for 3 days is 8.7 mg / g, 8.2 mg / g and 2 mg / g and is reached 2, 6 and 24 hours after administration.

Concentration in urine

The mean urinary concentration of levofloxacin after administration of 150 mg, 300 mg or 500 mg once daily is 44 mg / l, 91 mg / l and 200 mg / l and is reached 8-12 hours after administration.