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

Description

Levasept Composition
active substance: levofloxacin;

100 ml of solution contain levofloxacin hemihydrate in terms of levofloxacin 500 mg;

excipients: anhydrous glucose, concentrated hydrochloric acid, sodium hydroxide, water for injection.

Levasept Dosage form
Solution for infusion.

Basic physical and chemical properties: transparent solution of greenish-yellow color.

Levasept Pharmacotherapeutic group
Antibacterial agents for systemic use from the group of quinolones. Fluoroquinolones. ATX code J01M A12.

Levasept Pharmacodynamics
Levofloxacin is a broad-spectrum antibiotic from the group of quinolones, containing an active substance – levofloxacin. Levofloxacin, like other fluorinated quinolones, blocks bacterial DNA gyrase, as a result of which the function of bacterial DNA is disrupted. Levofloxacin is active against gram-positive and gram-negative pathogenic microorganisms, including strains resistant to penicillins, cephalosporins and / or aminoglycosides. The development of resistance can significantly affect the sensitivity of local strains to the drug, therefore, when prescribing a drug, it is advisable to take this information into account, especially in the case of severe infections. Levofloxacin has a wide spectrum of microorganisms in the wastes in vitro and in vivo: Enterococcus faecalis, Staphylococcus aureus methicilinchuvium, Staphylococcus Enter epidermidis, Streptococcus aerobacterus, Enterococcus pneumoniae, Streptococcus pneumoniae, Streptococcus epidermidis, Enterococcus pneumoniae, Streptococci Enterobacter sakazakii, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Klebsiella oxytoca, Legionella pneumopnia, Moraxella catarrhalis, Proteus mirabilis, Pseudomonas aeruginosa, Pseudomonas fluorescens, Chlamydophila pneumoniae, Mycoplasma pneumoniae, Acinetobacter anitratus, Acinetobacter baumannii, Acinetobacter calcoaceticus, Bordetella pertussis , Citrobacter diversus, Citrobacter freundii, Morganella morganii, Proteus vulgaris, Providencia rettgeri et stuartii, Serratia marcescens, Clostridium perfringens.

Like other fluoroquinolones, levofloxacin is inactive against spirochetes.

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

Suction. When taken orally, levofloxacin is rapidly and almost completely absorbed. The peak concentration in blood plasma is reached 1 hour after ingestion. Bioavailability is almost 100%. Levofloxacin is subject to linear pharmacokinetics in the range of 50-600 mg. Food intake somewhat affects the absorption of the drug.

Distribution.

About 30-40% of levofloxacin binds to serum protein. The cumulative effect of levofloxacin at a dosage of 500 mg once a day is practically absent. There is an insignificant, but supposed, its cumulation at a dosage of 500 mg 2 times a day. Stable distribution rates are achieved within 3 days.

Distribution in tissues and body fluids. Distribution in the bronchial mucosa and the secretion of the bronchial epithelium. The maximum concentration of levofloxacin in the bronchial mucosa and the secretion of the bronchial epithelium at a dose of 500 mg per os was 8.3 and 10.8 mg / ml, respectively.

Distribution into lung tissue. The maximum concentration of levofloxacin in the lung tissue at a dose of 500 mg per os was approximately 11.3 mg / ml and was reached within 4-6 hours after administration. The concentration in the lungs constantly exceeded that in the blood plasma.

Distribution in the cerebrospinal fluid. Levofloxacin poorly penetrates into the cerebrospinal fluid.

Distribution into prostate tissue. After taking 500 mg of levofloxacin once a day for 3 days, the average concentrations in the prostate tissue were 8.7 mg / g, 8.2 mg / g and 2 mg / g – after 2, 6 and 24 hours, respectively; the average concentration ratio in the prostate / plasma is 1.84.

Concentration in urine. The average concentration of levofloxacin within 8-12 hours after a single dose of 150 mg, 300 mg or 500 mg per os was 44 mg / ml, 91 mg / ml and 200 mg / ml, respectively.

Metabolism. Levofloxacin is metabolized to a very insignificant extent; the metabolites are dismethyl-levofloxacin and levofloxacin N-oxide. These metabolites make up less than 5% of the amount of the drug that is excreted in the urine.

Excretion. After oral administration, levofloxacin is excreted from blood plasma somewhat slowly (half-life is 6-8 hours). Withdrawal is carried out mainly by the kidneys (85% of the administered dose).

Indications
Bacterial inflammation caused by bacteria sensitive to the drug:

community-acquired pneumonia
complicated urinary tract infections, including acute pyelonephritis;
complicated infections of the skin and soft tissues (only if it is considered ineffective or inappropriate to use other antibacterial agents that are usually prescribed to treat these infections)
chronic bacterial prostatitis.
Should take into account official rivers