Levofloxacin, 10 pcs., 500 mg, film-coated tablets

Composition per tablet:

Description

Capsule-shaped biconvex tablets, film-coated, white or almost white; on the cross section two layers are visible, the inner layer is light yellow to yellow in color, white inclusions are allowed.

Pharmacotherapeutic group:

antimicrobial agent, fluoroquinolone.

ATX code:

J01MA12.

Pharmacological properties

Pharmacodynamics

Levofloxacin is a synthetic broad-spectrum antibacterial drug from the group of fluoroquinolones, containing the levorotatory isomer of ofloxacin as an active substance.

Levofloxacin blocks DNA gyrase, disrupts supercoiling and cross-linking of DNA breaks, inhibits DNA synthesis, and causes profound morphological changes in the cytoplasm, cell wall and membranes of bacteria.

Levofloxacin has a bactericidal effect and is active against a large number of pathogens of bacterial infections both in vitro

, and
in vivo
.

Sensitive microorganisms (minimum inhibitory concentration (MIC) ≤ 2 mg/l):

• aerobic gram-positive microorganisms: Bacillus anthracis , Corynebacterium diphtheriae , Corynebacterium jeikeium , Enterococcus spp
  ., including
  Enterococcus faecalis, Listeria monocytogenes, Staphylococcus spp.
  ( coagulase-negative, methicillin-sensitive/leukotoxin-containing/moderately sensitive strains), including
  Staphylococcus aureus (
  methicillin-sensitive strains
  ), Staphylococcus epidermidis (
  methicillin-sensitive strains
  ), Streptococcus spp.
  groups C and G, Streptococcus agalactiae, Streptococcus pneumoniae ( penicillin-sensitive / moderately sensitive / resistant strains
  ), Streptococcus pyogenes, Streptococcus spp.
  Viridans group ( penicillin-sensitive/resistant strains
  );
• aerobic gram-negative microorganisms: Acinetobacter spp .
  , including
  Acinetobacter baumannii , Acinetobacillus actinomycetemcomitans , Citrobacter freundii , Eikenella corrodens , Enterobacter spp
  ., including
  Enterobacter aerogenes , Enterobacter cloacae , Escherichia coli , Gardnerella vaginalis , Haemophilus ducreyi , Haemophilus influenzae
  (ampicillin-sensitive/ resistant strains),
  Haemophilus parainfluenzae , Helicobacter pylori , Klebsiella spp
  ., including
  Klebsiella oxytoca , Klebsiella pneumoniae , Moraxella catarrhalis
  (beta-lactamase producing and non-producing strains),
  Morganella morganii , Neisseria gonorrhoeae
  (penicillinase producing and non-producing strains),
  Neisseria meningitidis , Pasteurella spp .
  , including
  Pasteurella canis , Pasteurella dagmatis , Pasteurella multocida , Proteus mirabilis , Proteus vulgaris , Providencia spp
  ., including
  Providencia rettgeri , Providencia stuartii , Pseudomonas spp .
  , including
  Pseudomonas aeruginosa
  (hospital infections caused by
  Pseudomonas aeruginosa
  may require combination treatment),
  Serratia spp
  ., including
  Serratia marcescens , Salmonella spp
  .;
• anaerobic microorganisms: Bacteroides fragilis , Bifidobacterium spp ., Clostridium perfringens , Fusobacterium spp ., Peptostreptococcus spp ., Propionibacterium spp ., Veillonella spp
  .;
• other microorganisms: Bartonella spp ., Chlamydia pneumoniae , Chlamydia psittaci , Chlamydia trachomatis , Legionella pneumophila , Legionella spp ., Mycobacterium spp .
  , including
  Mycobacterium leprae , Mycobacterium tuberculosis , Mycoplasma hominis , Mycoplasma pneumoniae , Rickettsia spp ., Ureaplasma urealyticum
  .

Moderately sensitive microorganisms (MIC = 4 mg/l):

• aerobic gram-positive microorganisms: Corynebacterium urealyticum , Corynebacterium xerosis , Enterococcus faecium , Staphylococcus epidermidis
  (methicillin-resistant strains),
  Staphylococcus haemolyticus
  (methicillin-resistant strains);
• aerobic gram-negative microorganisms: Campylobacter jejuni , Campylobacter coli
  ;
• anaerobic microorganisms: Prevotella spp ., Porphyromonas spp
  .

Resistant microorganisms (MIC more than 8 mg/l):

• aerobic gram-positive microorganisms: Staphylococcus aureus
  (methicillin-resistant strains), other
  Staphylococcus spp
  . (coagulase-negative methicillin-resistant strains);
• aerobic gram-negative microorganisms: Alcaligenes xylosoxidans
  ;
• anaerobic microorganisms: Bacteroides thetaiotaomicron
• other microorganisms: Mycobacterium avium
  .

Clinical efficacy (effectiveness in clinical studies against infections caused by the following microorganisms):

• aerobic gram-positive microorganisms: Enterococcus faecalis , Staphylococcus aureus , Streptococcus pneumoniae , Streptococcus pyogenes
  ;
• aerobic gram-negative microorganisms: Citrobacter freundii , Enterobacter cloacae , Escherichia coli , Haemophilus influenzae , Haemophilus parainfluenzae , Klebsiella pneumoniae , Moraxella catarrhalis , Morganella morganii , Proteus mirabilis , Pseudomonas aeruginosa , Serratia marcescens
  ;
• other microorganisms: Chlamydia pneumoniae , Legionella pneumophila , Mycoplasma pneumoniae
  .

Resistance to levofloxacin develops as a result of a stepwise process of mutations in the genes encoding both type II topoisomerases: DNA gyrase and topoisomerase IV. Other resistance mechanisms, such as the mechanism of influencing the penetration barriers of the microbial cell (a mechanism characteristic of Pseudomonas
aeruginosa
) and the mechanism of efflux (active removal of the antimicrobial agent from the microbial cell), may also reduce the sensitivity of microorganisms to levofloxacin.

Due to the peculiarities of the mechanism of action of levofloxacin, cross-resistance between levofloxacin and other antimicrobial agents is not usually observed.

Farmakok u no u ka

Absorption

Levofloxacin is rapidly and almost completely absorbed after oral administration; food intake has little effect on its absorption. Absolute bioavailability when taken orally is 99-100%. After a single dose of 500 mg of levofloxacin, the maximum concentration in blood plasma (Cmax) is reached within 1-2 hours and is 5.2 ± 1.2 μg/ml. The pharmacokinetics of levofloxacin is linear in the dose range from 50 to 1000 mg. The equilibrium state of levofloxacin concentration in blood plasma when taking 500 mg of levofloxacin 1 or 2 times a day is achieved within 48 hours.

On the 10th day of oral administration of the drug Levofloxacin Ecolevid® 500 mg 1 time per day, the Cmax of levofloxacin was 5.7 ± 1.4 mcg/ml, and the minimum concentration of levofloxacin (concentration before taking the next dose) (Cmin) in the blood plasma was 0.5 ±0.2 µg/ml.

On the 10th day of oral administration of the drug Levofloxacin Ecolevid® 500 mg 2 times a day, Cmax was 7.8 ± 1.1 μg/ml, and C min was 3.0 ± 0.9 μg/ml.

Distribution

The connection with serum proteins is 30-40%. After a single and repeated dose of 500 mg of levofloxacin, the volume of distribution of levofloxacin is, on average, 100 l, which indicates good penetration of levofloxacin into organs and tissues of the human body.

Penetration into the bronchial mucosa, epithelial lining fluid, alveolar macrophages

After a single oral dose of 500 mg of levofloxacin, the maximum concentrations of levofloxacin in the bronchial mucosa and epithelial lining fluid were reached within 1 hour or 4 hours and were 8.3 μg/g and 10.8 μg/ml, respectively, with penetration coefficients into the mucosa bronchi and epithelial lining fluid, compared with plasma concentrations of 1.1-1.8 and 0.8-3, respectively.

After 5 days of oral administration of 500 mg levofloxacin, the mean concentrations of levofloxacin 4 hours after the last dose in the epithelial lining fluid were 9.94 μg/ml and in alveolar macrophages - 97.9 μg/ml.

Penetration into lung tissue

Maximum concentrations in lung tissue after oral administration of 500 mg of levofloxacin were approximately 11.3 mcg/g and were achieved 4-6 hours after dosing with penetration coefficients of 2-5, compared with plasma concentrations.

Penetration into alveolar fluid

After 3 days of taking 500 mg of levofloxacin 1 or 2 times a day, the maximum concentrations of levofloxacin in the alveolar fluid were reached 2-4 hours after taking the drug and were 4.0 and 6.7 μg/ml, respectively, with a penetration coefficient of 1. compared to plasma concentrations.

Penetration into bone tissue

Levofloxacin penetrates well into cortical and cancellous bone tissue in both the proximal and distal parts of the femur, with a penetration coefficient (bone tissue/blood plasma) of 0.1-3. The maximum concentrations of levofloxacin in the cancellous bone tissue of the proximal femur after oral administration of 500 mg of the drug were approximately 15.1 mcg/g (2 hours after dosing).

Penetration into the cerebrospinal fluid

Levofloxacin penetrates poorly into the cerebrospinal fluid.

Penetration into prostate tissue

After oral administration of 500 mg of levofloxacin once daily for 3 days, the average concentration of levofloxacin in prostate tissue was 8.7 mcg/g, the average prostate/blood plasma concentration ratio was 1.84.

Concentrations in urine

Mean urinary concentrations 8 to 12 hours after oral doses of 150, 300, and 600 mg of levofloxacin were 44 mcg/mL, 91 mcg/mL, and 162 mcg/mL, respectively.

Metabolism

Levofloxacin is metabolized to a small extent (5% of the dose taken). Its metabolites are demethyllevofloxacin and levofloxacin N-oxide, which are excreted by the kidneys. Levofloxacin is stereochemically stable and does not undergo chiral transformations.

Removal

After oral administration, levofloxacin is relatively slowly eliminated from the blood plasma (half-life (T1/2) - 6-8 hours). Excretion is mainly through the kidneys (more than 85% of the dose taken). The total clearance of levofloxacin after a single dose of 500 mg was 175±29.2 ml/min.

There are no significant differences in the pharmacokinetics of levofloxacin when administered intravenously and orally, which confirms that oral and intravenous administration are interchangeable.

Pharmacokinetics in selected patient groups

The pharmacokinetics of levofloxacin do not differ between men and women.

Pharmacokinetics in elderly patients do not differ from those in younger patients, with the exception of differences in pharmacokinetics associated with differences in creatinine clearance (CC).

In renal failure, the pharmacokinetics of levofloxacin changes. As renal function deteriorates, renal excretion and renal clearance (CIR) decrease and T1/2 increases.

Pharmacokinetics in renal failure after a single oral dose of 500 mg of Levofloxacin Ecolevid®.

Indications for use

Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to levofloxacin:

• community-acquired pneumonia;
• complicated urinary tract infections and pyelonephritis;
• chronic bacterial prostatitis;
• infections of the skin and soft tissues;
• for complex treatment of drug-resistant forms of tuberculosis;
• prevention and treatment of anthrax through airborne transmission.

For the treatment of the following infectious and inflammatory diseases, levofloxacin can be used as an alternative to other antimicrobial drugs:

• acute sinusitis;
• exacerbation of chronic bronchitis;
• uncomplicated cystitis.

When using the drug Levofloxacin Ecolevid®, official national recommendations on the proper use of antibacterial drugs, as well as the sensitivity of pathogenic microorganisms in a particular country should be taken into account (see section "Special instructions").

Levofloxacin or Ciprofloxacin – which is better and more effective?

Manufacturer: RAFARMA, Russia
Release form: tablets, eye drops

Active ingredient: ciprofloxacin

Ciprofloxacin is a prescription analogue of Levofloxacin with the same active ingredient in the composition. This is an antimicrobial drug with a broad spectrum of action that has a bactericidal effect.

It has a detrimental effect on most pathogens that provoke infectious and inflammatory pathologies of the respiratory tract, abdominal cavity, pelvic organs, bone and joint tissue.

It is also prescribed for patients of the older age group for septicemia and diseases in otolaryngology. Ciprofloxacin can be used as a prophylactic against infections in immunocompromised patients, as well as for prostatitis in men.

To achieve maximum results from therapy, you must adhere to the prescribed dosage and course duration.

Contraindications

Hypersensitivity to levofloxacin, other fluoroquinolones or components of the drug, epilepsy, tendon damage during previous treatment with quinolones, pregnancy, lactation, childhood and adolescence (up to 18 years), myasthenia gravis.

Lactose intolerance or lactase deficiency, as well as glucose-galactose malabsorption.

Due to the inability to split the tablet in two, the use of the drug is contraindicated in patients with impaired renal function:

• in patients with creatinine clearance less than 50 ml/min, it is impossible to use a dosage regimen with an initial dosage of 250 mg/24 hours;
• in patients with creatinine clearance less than 20 ml/min, it is impossible to use the dosage regimen with an initial dosage of 500 mg/24 hours and 500 mg/12 hours;
• when creatinine clearance is less than 10 ml/min (including during hemodialysis and continuous ambulatory peritoneal dialysis), it is impossible to use it for all dosage regimens.

Levofloxacin analogs

On pharmacy shelves there is an assortment of foreign and Russian analogues of Levofloxacin in ampoules, tablets, and also in the form of eye drops. When choosing an identical substitute, you should pay attention to products that are similar in composition (active ingredient). The main differences between the products are the manufacturer, price category and pharmacological action. Most drugs are available by prescription, so it is recommended that you first seek additional advice from a specialist to make an accurate diagnosis and eliminate restrictions.

List of Levofloxacin analogues with prices

Carefully

• In patients predisposed to the development of seizures [in patients with previous lesions of the central nervous system (CNS); in patients simultaneously taking drugs that lower the threshold of convulsive activity of the brain, such as fenbufen, theophylline] (see section “Interaction with other drugs”);
• In patients with latent or manifest deficiency of glucose-6-phosphate dehydrogenase (increased risk of hemolytic reactions during treatment with quinolones);
• In patients with impaired renal function (mandatory monitoring of renal function is required, as well as correction of the dosage regimen, see section “Dosage and Administration”);
• In patients with known risk factors for QT interval prolongation: in elderly patients; in female patients; in patients with uncorrected electrolyte disturbances (with hypokalemia, hypomagnesemia); with congenital long QT syndrome; with heart disease (heart failure, myocardial infarction, bradycardia); while taking medications that can prolong the QT interval (class IA and III antiarrhythmic drugs, tricyclic antidepressants, macrolides, antipsychotics) (see sections “Overdose”, “Interaction with other drugs”, “Special instructions”);
• In patients with diabetes mellitus receiving oral hypoglycemic drugs (for example, glibenclamide) or insulin drugs (the risk of hypoglycemia increases);
• In patients with severe adverse reactions to other fluoroquinolones, such as severe neurological reactions (increased risk of developing similar adverse reactions when using levofloxacin);
• In patients with psychosis or in patients with a history of mental illness (see section "Special instructions");
• In elderly patients, in patients after transplantation, as well as with concomitant use of glucocorticosteroids (increased risk of tendinitis and tendon rupture) (see section "Special instructions").

Answers on questions

Is Levofloxacin an antibiotic or not?

It is an antibacterial and antimicrobial drug. Therefore, during the course it is necessary to take probiotics to restore intestinal microflora.

Can I take levofloxacin with alcohol or not?

Levofloxacin is incompatible with alcoholic beverages.

Is Levofloxacin an antibiotic or an antiviral?

The medication is not an antiviral drug, it is an antibiotic.

Directions for use and doses

Inside. Once or twice a day. The tablets should be swallowed without chewing and washed down with a sufficient amount of liquid (0.5 to 1 glass).

The drug can be taken before meals or at any time between meals, since food intake does not affect the absorption of the drug (see section "Pharmacokinetics").

The drug should be taken at least 2 hours before or 2 hours after taking drugs containing magnesium and/or aluminum, iron, zinc, or sucralfate (see section “Interaction with other drugs”).

Considering that the bioavailability of levofloxacin when taking Levofloxacin Ecolevid® tablets is 99-100%, if the patient is transferred from intravenous infusion with other levofloxacin drugs, taking Levofloxacin Ecolevid® tablets should be continued at the same dose that was used for intravenous infusion of levofloxacin drugs (see section "Pharmacokinetics").

Skipping one or more doses of the drug

If you accidentally miss a dose of the drug, you should take the next dose as soon as possible and then continue to take Levofloxacin Ecolevid® according to the recommended dosage regimen.

Levofloxacin or Ceftriaxone – which is better and more effective for pneumonia

Manufacturer: PHARMSTANDARD+, Russia
Release form: powder for the preparation of solution for injection

Active ingredient: ceftriaxone

Ceftriaxone is an analogue of Levofloxacin infusion solution, which is even prescribed to women during pregnancy, but only in the second and third trimester. The drug is classified as a third generation cephalosporin antibiotic. The drug has bactericidal properties.

A new generation analogue of Levofloxacin injections is prescribed to patients with infectious pathologies of the respiratory tract, skin, genitourinary system, bone, joint and connective tissue. Used in otolaryngology. The drug is also prescribed as a prophylaxis after surgery.