Levofloxacin pills 500mg, 10pcs – Biochemist

Composition

For one 500 mg tablet:

Active ingredient: levofloxacin hemihydrate-512.46 mg, in terms of levofloxacin-500.00 mg;

Excipients of the tablet core: povidone (kollidon 30) – 25,80 mg, microcrystalline cellulose – 182,54 mg, magnesium stearate – 8,00 mg crospovidone (kollidon CL) – 35,20 mg, sodium lauryl sulfate – 16,00 mg; excipients film shell: hypromellose – of 11.56 mg, macrogol 6000 – 4,70 mg, titanium dioxide – 1,78 mg, Polysorbate 80 to 1.78 mg, dye quinoline yellow E 104-0,18 mg.

Pharmacological action

Pharmacodynamics

A synthetic broad-spectrum antibacterial drug from the group of fluoroquinolones containing levofloxacin, a levorotatory isomer of ofloxacin, as the Active ingredient.

Levofloxacin blocks DNA gyrase and topoisomerase IV, disrupts supercoiling and crosslinking of DNA breaks, inhibits DNA synthesis, and causes deep morphological changes in the cytoplasm, cell wall, and membranes of microbial cells.

Levofloxacin is active against most strains of microorganisms, both in vitro and in vivo.

In vitro

susceptible organisms (IPC < 2 mg/l; zone of inhibition of >17 mm)

– Aerobic gram-positive microorganisms: Bacillus anthracis, Corynebacterium diphtheriae, Corynebacterium jeikeium, Enterococcus faecalis, Enterococcus spp., Listeria monocytogenes, Staphylococcus coagulase-negative methi-S(I) [coagulasenegative methicillin-sensitive/-moderately sensitive)], Staphylococcus aureus methi-S (methicillin – susceptible), Staphylococcus epidermidis methi-S (methicillin-susceptible), Staphylococcus spp. CNS (coagulase-negative), Streptococci of groups C and G, Streptococcus agalactiae, Streptococcus pneumoniae peni I/S/R (penicillin-moderately sensitive/ – sensitive/ – resistant), Streptococcus pyogenes, Viridans streptococci peni-S/R (penicillin-sensitive/ – resistant).

– Aerobic gram-negative microorganisms: Acinetobacter baumannii, Acinetobacter spp., Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter cloacae, Enterobacter spp., Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae ampi-S/R (ampicillin-sensitive/resistant), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella oxytoca, Klebsiella pneumoniae, Klebsiella spp., Moraxella catarrhalis β+/β- (reproducirse and producing beta-lactamase), Morganella morganii, Neisseria gonorrhoeae pop PPNG/PPNG (reproducirse and producing penicillinase), Neisseria meningitidis, Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida, Pasteurella spp., Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Providencia spp., Pseudomonas aeruginosa (hospital infections caused by Pseudomonas aeruginosa may require combined treatment), Pseudomonas spp., Salmonella spp. Serratia marcescens, Serratia spp.

– Anaerobic microorganisms: Bacteroides Jragilis, Bifidobacterium spp., Clostridium perfringens, Eusobacterium spp. Peptostreptococcus, Propionibacterium spp., Veillonella spp.

– Other microorganisms: Bartonella spp. Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella pneumophila, Legionella spp., Mycobacterium spp. Mycobacterium leprae, Mycobacterium tuberculosis, Mycoplasma hominis, Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum.

Moderately sensitive microorganisms (MPC = 4 mg / l; inhibition zone 16-14 mm)

– Aerobic gram-positive microorganisms: Corynebacterium urealyticum. Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermic/is methi-R (methicillin-resistant), Staphylococcus haemolyticus methi-R (methicillin – resistant).

– Aerobic gram-negative microorganisms: Campylobacter jejuni / coli.

– Anaerobic microorganisms: Prevotella spp., Porphyromonas spp.

Levofloxacin-resistant microorganisms (MPC > 8 mg / l; inhibition zone ≤13 mm)>

– Aerobic gram-positive microorganisms: Staphylococcus aureus methi-R (methicillin-resistant), Staphylococcus coagulase-negative methi-R (coagulase-negative methicillin-resistant).

– Aerobic gram-negative microorganisms: Alcaligenes xylosoxidans.

– Anaerobic microorganisms: Bacteroides thetaiotaomicron.

– Other microorganisms: Mycobacterium avium.

Clinical efficacy

In clinical studies, the drug was effective in treating 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 (Branhamella) catarrhalis, Morganella morganii, Proteus mirabilis, Pseudomonas aeruginosa, Serratia marcescens.

Others: Chlamydia pneumoniae, Legionella pneumophila, Mycoplasma pneumoniae.

Resistance

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

Due to the specific mechanism of action of levofloxacin, there is usually no cross-resistance between levofloxacin and other antimicrobial agents.

Pharmacokinetics

Absorption rate

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

On day 10 of oral use of 500 mg once a day_{, the cmax} of levofloxacin was 5.7±1.4 mcg / ml, and the minimum concentration of levofloxacin (concentration before taking the next dose) (C_min) in blood plasma was 0.5±0.2 mcg/ml.

On day 10 of oral use of Levofloxacin 500 mg 2 times a day, the_cmax

was 7.8±1.1 mcg / ml, and the_cmin was 3.0±0.9 mcg/ml.

Distribution

The relationship with serum proteins is 30-40%. After a single and repeated use of 500 mg of the drug, the volume of distribution of levofloxacin averages 100 liters, which indicates a good penetration of levofloxacin into the 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 the drug, the maximum concentrations of levofloxacin in the bronchial mucosa and epithelial lining fluid were reached within 1 hour or 4 hours and amounted to 8.3 mcg/g and 10.8 mcg / ml, respectively, with penetration coefficients into the bronchial mucosa and epithelial lining fluid compared to plasma concentrations of 1.1-1.8 and 0.8-3, respectively.

After 5 days of oral use of 500 mg of the drug, the average concentrations of levofloxacin 4 hours after the last dose of the drug in the fluid of the epithelial lining were 9.94 mcg/ml and in alveolar macrophages – 97.9 mcg/ml.

Penetration of lung tissue

Maximum concentrations in the lung tissue after oral use of 500 mg of levofloxacin were approximately 11.3 mcg/g and reached 4-6 hours after taking the drug with penetration coefficients 2-5 compared to the concentration in blood plasma.

Penetration into the alveolar fluid

After 3 days of taking 500 mg of the drug 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 micrograms / ml, respectively, with a penetration coefficient of 1 compared to blood plasma concentrations. Bone penetration

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

Penetration into the cerebrospinal fluid

Levofloxacin does not penetrate well into the cerebrospinal fluid.

Penetration of prostate tissue

After oral use of 500 mg of the drug once a day for 3 days, the average concentration of levofloxacin in the prostate tissue was 8.7 mcg/g, the average ratio of prostate / blood plasma concentrations was 1.84.

Concentrations in the urine

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

Metabolism

Levofloxacin is only slightly metabolized (5% of the dose taken). Its metabolites are desmethylvofloxacin and N-oxide levofloxacin, which are excreted by the kidneys. Levofloxacin is stereochemically stable and does not undergo chiral transformations. Deduction

After oral use, levofloxacin is relatively slowly eliminated from the blood plasma (half-life (T_1/2) – 6-8 hours). Excretion mainly through the kidneys (more than 85% of the dose taken). The total clearance of levofloxacin after a single 500 mg dose was 175±29.2 ml/min.

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

Pharmacokinetics in individual groups of patients

, the pharmacokinetics of levofloxacin in men and women do not differ. Pharmacokinetics in elderly patients do not differ from those in young patients, with the exception of pharmacokinetic differences associated with differences in creatinine clearance (CC).

In patients with renal insufficiency, the pharmacokinetics of levofloxacin are altered. As renal function worsens, renal excretion and clearance decrease, and T_1/2 increases.

Pharmacokinetics in renal insufficiency after a single oral dose of 500 mg of levofloxacin

KK (ml / min)	<20	20-49
Renal clearance (ml / min)	13	26
T1/2 (h)	35	27

Indications

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 the complex treatment of drug-resistant forms of tuberculosis;

– prevention and treatment of anthrax in the airborne pathway of infection.

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 levofloxacin, you should take into account the official national guidelines for the proper use of antibacterial agents, as well as the sensitivity of pathogens in a particular country.

Use during pregnancy and lactation

The use of Levofloxacin is contraindicated in pregnant and breast-feeding women.

Contraindications

-Hypersensitivity to levofloxacin or other quinolones, as well as to any of the excipients of Levofloxacin.

– Epilepsy.

– Pseudoparalytic myasthenia gravis (see sections “Side effects”, “Special instructions”),

– A history of tendon damage when taking fluoroquinolones.

– Children and adolescents under 18 years of age (due to incomplete growth of the skeleton, since the risk of damage to cartilage growth points cannot be completely excluded).

– Pregnancy (the risk of damage to cartilage growth points in the fetus cannot be completely excluded).

– The period of breastfeeding (the risk of damage to the cartilage points of bone growth in the child cannot be completely excluded).

– In patients with creatinine clearance less than 50 ml/min cannot be used in the dosing regimen with an initial dose of 250 mg/24 h in patients with creatinine clearance less than 20 ml/min cannot be used in the dosing regimen with an initial dose of 500 mg/24 h and 500 mg/12 hours (including during hemodialysis and continuous ambulatory peritoneal dialysis) cannot apply for all dosing regimens.

Caution

– patients predisposed to the development of seizures [patients with precursor lesions of the Central nervous system (CNS) in patients concurrently taking drugs that reduce the threshold of convulsive readiness of the brain, such as fenbufen, theophylline] (see section “Interaction with other drugs”),

– in patients with latent or manifestating deficiency of glucose-6 – phosphate dehydrogenase (increased risk of hemolytic reactions in the treatment chinaonly).

– Patients with known risk factors for QT interval prolongation: patients of advanced age; in female patients, patients with uncorrected electrolyte disorders (hypokalemia with a hypomagnesemia), a syndrome of congenital QT prolongation; cardiac (heart failure, myocardial infarction, bradycardia); the simultaneous use of drugs that can prolong the QT interval (antiarrhythmic agents class IA and III, tricyclic antidepressants, macrolides, antipsychotics) (see sections on “Overdose”, “Interaction with other medicinal products”, the “Special instructions”).

– In patients with diabetes mellitus who take oral hypoglycemic drugs, such as glibenclamide or insulin preparations (the risk of hypoglycemia increases).

– In patients with severe adverse reactions to other fluoroquinolones, such as severe neurological reactions (increased risk of similar adverse reactions with levofloxacin).

– In patients with psychosis or in patients with a history of mental illness (see section “Special instructions”).

– In patients with impaired renal function with a creatinine clearance of 50-20 ml / min (see section “Contraindications”),

In elderly patients, in patients after transplantation, as well as with concomitant use of glucocorticosteroids (increased risk of tendinitis and tendon rupture) (see the section “Special instructions”).

Side effects

The following side effects are presented according to the following frequency gradations: very common (>1/10); common (>>1/100, >><1/10); infrequently (>1/1000, <1/10); infrequently (><1/100); rarely (>1/10000, <1/100); rarely (><1/1000); very rarely (

Infectious and parasitic diseases

Infrequently: fungal infections, development of resistance of pathogenic microorganisms.

Disorders of the blood and lymphatic system Infrequently: leukopenia (a decrease in the number of white blood cells in the peripheral blood), eosinophilia (an increase in the number of eosinophils in the peripheral blood);

Rare: neutropenia (decrease in the number of neutrophils in the peripheral blood), thrombocytopenia (decrease in the number of platelets in the peripheral blood);

Frequency unknown: pancytopenia (decrease in the number of all formed elements in the peripheral blood), agranulocytosis (absence or sharp decrease in the number of granulocytes in the peripheral blood), hemolytic anemia.

Immune system disorders

Rare: angioedema;

Frequency unknown: anaphylactic shock, anaphylactoid shock. Anaphylactic and anaphylactoid reactions can sometimes develop even after taking the first dose of the drug.

Metabolic and nutritional disorders

Infrequently: anorexia;

Rare: hypoglycemia, especially in patients with diabetes mellitus (possible signs of hypoglycemia: “wolfish” appetite, nervousness, perspiration, trembling). Frequency unknown: hyperglycemia, severe hyperglycemia, up to the development of hypoglycemic coma, especially in elderly patients, patients with diabetes mellitus taking oral hypoglycemic drugs or insulin.

Mental disorders

Often: insomnia;

Infrequently: feelings of restlessness, anxiety, confusion; Rarely: mental disorders (e. g. hallucinations, paranoia), depression, agitation (agitation), sleep disorders, nightmares; Frequency unknown: mental disorders with behavioral disorders with self-harm, including suicidal thoughts and suicide attempts, attention disorders, disorientation, nervousness, memory disorders, delirium.

Nervous system disorders

Often: headache, dizziness;

Infrequently: drowsiness, tremor, dysgeusia (taste distortion); Rarely: paresthesia, convulsions (see section “Special instructions”); Frequency unknown: peripheral sensory neuropathy, peripheral sensory-motor neuropathy (see section “Special Instructions”), dyskinesia, extrapyramidal disorders, ageusia (loss of taste sensations), parosmia (odour sensation disorder, especially subjective odour sensation, objectively absent), including loss of taste sensation. sense of smell; fainting, increased intracranial pressure (benign intracranial hypertension, pseudotumor).

Visual disturbances

Rare: visual disturbances, such as blurred vision;

Frequency unknown: transient vision loss, uveitis.

Hearing disorders and labyrinth disorders

Infrequently: vertigo (feeling of deflection or whirling, or of one’s own body or surrounding objects).

Rare: tinnitus;

Frequency unknown: hearing loss, hearing loss.

Cardiac disorders

Rare: sinus tachycardia, palpitation sensation;

Frequency unknown: prolongation of the QT interval, ventricular arrhythmias, ventricular tachycardia, polymorphic ventricular tachycardia of the “pirouette” type, which can lead to cardiac arrest (see sections “Overdose”, “Special instructions”).

Vascular disorders

Rare: low blood pressure.

Respiratory, thoracic and mediastinal disorders

Infrequently: shortness of breath;

Frequency unknown, bronchospasm, allergic pneumonitis.

Disorders of the gastrointestinal tract

Often: diarrhea, vomiting, nausea;

Infrequently: abdominal pain, dyspepsia, flatulence, constipation;

Frequency unknown: hemorrhagic diarrhea, which in very rare cases can be a sign of enterocolitis, including pseudomembranous colitis (see section “Special instructions”), pancreatitis, stomatitis.

Liver and biliary tract disorders

are common: increased activity of “liver” enzymes in the blood (for example, alanine aminotransferase (ALT), aspartate aminotransferase (ACT)), increased activity of alkaline phosphatase (ALP) and gamma-glutamyltransferase (GGT) in the blood;

Infrequently: increased blood bilirubin concentration;

frequency unknown: severe hepatic insufficiency, including cases of acute hepatic insufficiency, sometimes fatal, especially in patients with a severe underlying disease (for example, in patients with sepsis) (see the section “Special instructions”); hepatitis, jaundice.

Skin and subcutaneous tissue disorders

Infrequently: skin rash, pruritus, urticaria, hyperhidrosis;

Frequency unknown: toxic epidermal necrolysis, Stevens-Johnson syndrome, exudative erythema multiforme, photosensitization reactions (hypersensitivity to sunlight and ultraviolet radiation) (see section “Special instructions”), leukocytoclastic vasculitis.

Reactions from the skin and mucous membranes can sometimes develop even after taking the first dose of the drug.

Musculoskeletal and connective tissue disorders

Infrequently: arthralgia, myalgia;

Rare: tendon involvement, including tendinitis (e. g. Achilles tendon), muscle weakness, which may be particularly dangerous in patients with pseudoparalytic myasthenia gravis (see section “Special instructions”);

Frequency unknown: rhabdomyolysis, tendon rupture (e. g. Achilles tendon. This side effect may occur within 48 hours after starting treatment and may be bilateral in nature( see also the section “Special instructions”), ligament rupture, muscle rupture, arthritis.

Kidney and urinary tract disorders

Infrequently: increased serum creatinine;

Rare: acute renal failure (for example, due to the development of interstitial nephritis).

General disorders and disorders at the injection site

Infrequently: asthenia;

Rare: pyrexia (fever);

Frequency unknown: pain (including pain in the back, chest, and extremities).

Other possible undesirable effects related to all fluoroquinolones

Very rare: attacks of porphyria (a very rare metabolic disease) in patients with porphyria.

Interaction

Interactions that require caution

With preparations containing magnesium, aluminum, iron and zinc, didanosine

Drugs containing divalent or trivalent cations, such as zinc or iron salts (drugs for the treatment of anemia), magnesium – and/or aluminum-containing drugs (such as antacids), didanosine (only dosage forms containing aluminum or magnesium as a buffer), it is recommended to take at least 2 hours before or 2 hours after taking Levofloxacin.

Calcium salts have a minimal effect on the absorption of levofloxacin when taken orally.

With sucralfate

The effect of Levofloxacin is significantly weakened with the simultaneous use of sucralfate (a means to protect the gastric mucosa). Patients receiving levofloxacin and sucralfate are advised to take sucralfate 2 hours after taking levofloxacin.

No pharmacokinetic interaction of levofloxacin with theophylline was detected with theophylline, fenbufen or similar drugs from the group of nonsteroidal anti-inflammatory drugs (NSAIDs) that reduce the threshold of convulsive readiness of the brain

. However, with the simultaneous use of quinolones and theophylline, NSAIDs and other drugs that reduce the threshold of convulsive readiness of the brain, a pronounced decrease in the threshold of convulsive readiness of the brain is possible.

The concentration of levofloxacin with simultaneous use of fenbufen increases only by 13%.

With indirect anticoagulants (vitamin K antagonists)

Patients treated with levofloxacin in combination with indirect anticoagulants (for example, warfarin) experienced an increase in prothrombin time/international normalized ratio (MHO) and/or the development of bleeding, including severe bleeding. Therefore, with the simultaneous use of indirect anticoagulants and levofloxacin, regular monitoring of blood clotting parameters is necessary.

With probenecid and cimetidine

Caution should be exercised when concomitantly using medications that interfere with renal tubular secretion, such as probenecid and cimetidine, and levofloxacin, especially in patients with renal insufficiency. Elimination (renal clearance)of levofloxacin is slowed by cimetidine by 24% and probenecid by 34%. It is unlikely that this can be of clinical significance in normal renal function.

With cyclosporine

Levofloxacin increased cyclosporine T1 / 2 by 33%. Since this increase is clinically insignificant, no dose adjustment of cyclosporine is required when it is co-administered with levofloxacin. With glucocorticosteroids

Concomitant use of glucocorticosteroids increases the risk of tendon rupture.

With medications that prolong the QT interval, Levofloxacin, like other fluoroquinolones, should be used with caution in patients receiving drugs that prolong the QT interval (for example, Class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, neuroleptics).

Other combinations

Clinical and pharmacological studies conducted to study possible pharmacokinetic interactions of levofloxacin with digoxin, glibenclamide, ranitidine and warfarin have shown that the pharmacokinetics of levofloxacin when used concomitantly with these drugs do not change sufficiently to have clinical significance.

How to take, course of use and dosage

Dosage regimen

Levofloxacin 250 mg or 500 mg is taken orally once or twice a day. Levofloxacin should be swallowed without chewing and washed down with a sufficient amount of liquid (from 0.5 to 1 cup). If necessary, the drug Levofloxacin 500 mg can be broken down according to the risk. Levofloxacin can be taken before meals or at any time between meals, since simultaneous food intake does not affect the absorption of the drug (see the section “Pharmacokinetics”). Levofloxacin should be taken at least 2 hours before or 2 hours after taking medications containing magnesium and / or aluminum, iron, zinc, or sucralfate (see the section “Interaction with other medications”).

Given that the bioavailability of levofloxacin when taking the drug in tablets is 99-100%, if the patient is transferred from intravenous use of Levofloxacin to taking tablets, treatment should continue at the same dose that was used for intravenous use (see the section “Pharmacokinetics”).

Dosage and duration of treatment

The dosage regimen is determined by the nature and severity of the infection, as well as the sensitivity of the suspected pathogen. The duration of treatment varies depending on the course of the disease.

Recommended dosage regimen and duration of treatment in patients with normal renal function (KK >50 ml / min)

Community-acquired pneumonia: 2 tablets of Levofloxacin 250 mg or 1 tablet of Levofloxacin 500 mg 1-2 times a day (respectively,500-1000 mg of levofloxacin) – 7-14 days.

– Complicated urinary tract infections: 2 tablets of Levofloxacin 250 mg once a day or 1 tablet of Levofloxacin 500 mg once a day (respectively,500 mg of levofloxacin) – 7-14 days.

– Pyelonephritis: 2 tablets of Levofloxacin 250 mg 1 time a day or 1 tablet of Levofloxacin 500 mg 1 time a day (respectively,500 mg of levofloxacin) – 7-10 days.

– Chronic bacterial prostatitis: 2 tablets of Levofloxacin 250 mg or 1 tablet of Levofloxacin 500 mg once a day (respectively,500 mg of levofloxacin) – 28 days.

– Infections of the skin and soft tissues: 2 tablets of Levofloxacin 250 mg or 1 tablet of Levofloxacin 500 mg 1-2 times a day (respectively,500-1000 mg of levofloxacin) – 7-14 days.

– Complex treatment of drug-resistant forms of tuberculosis: 1 tablet of Levofloxacin 500 mg 1-2 times a day (respectively,500-1000 mg of levofloxacin) – up to 3 months.

– Prevention and treatment of anthrax with airborne infection: 2 tablets of Levofloxacin 250 mg or 1 tablet of Levofloxacin 500 mg (respectively,500 mg of levofloxacin) 1 time a day for up to 8 weeks.

– Acute sinusitis: 2 tablets of Levofloxacin 250 mg or 1 tablet of Levofloxacin 500 mg once a day (respectively,500 mg of levofloxacin) – 10-14 days.

– Exacerbation of chronic bronchitis: 2 tablets of Levofloxacin 250 mg or 1 tablet of LevofloxacinCases of liver necrosis, including fatal liver failure, have been reported with levofloxacin, mainly in patients with severe underlying medical conditions, such as sepsis (see section “Adverse effects”). Patients should be warned to stop treatment and seek immediate medical attention if signs and symptoms of liver damage appear, such as anorexia, jaundice, dark urine, itching, and abdominal pain.

Patients with renal insufficiency

Since levofloxacin is mainly excreted through the kidneys, patients with impaired renal function require mandatory monitoring of renal function, as well as correction of the dosage regimen (see the section “Dosage and use”). When treating elderly patients, it should

be borne in mind that patients in this group often have impaired renal function (see the section “Dosage and use”). Prevention of photosensitization reactions Although photosensitization is very rare with levofloxacin, to prevent its development, patients are not recommended to be exposed unnecessarily to strong solar or artificial ultraviolet radiation (for example, to visit a tanning salon) during treatment and within 48 hours after the end of treatment with levofloxacin.

Superinfection

As with other antibiotics, the use of levofloxacin, especially for a long time, can lead to increased reproduction of microorganisms that are insensitive to it (bacteria and fungi), which can cause changes in the microflora that is normally present in humans. As a result, superinfection may develop. Therefore, during treatment, it is necessary to re-evaluate the patient’s condition and if superinfection develops during treatment, appropriate measures should be taken.

Prolongation of the QT interval

Very rare cases of QT prolongation have been reported in patients taking fluoroquinolones, including levofloxacin.

Caution should be exercised when using fluoroquinolones, including levofloxacin, in patients with known risk factors for prolongation of the QT interval: in patients with uncorrected electrolyte disturbances (hypokalemia, hypomagnesemia); with congenital QT prolongation syndrome; with heart diseases (heart failure, myocardial infarction, bradycardia); while taking medications that can prolong the QT interval, such as class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, antipsychotics.

Elderly and female patients may be more sensitive to drugs that prolong the QT interval. Therefore, fluoroquinolones, including levofloxacin, should be used with caution (see sections “With caution”, “Dosage and use”, “Side effects”, “Overdose” and “Interaction with other drugs”).

Patients with glucose-6-phosphate dehydrogenase deficiency

Patients with latent or manifest glucose-6 – phosphate dehydrogenase deficiency have a predisposition to develop hemolytic reactions during treatment with quinolones, which should be taken into account when treating with levofloxacin.

Hypo – and hyperglycemia (dysglycemia)

As with other quinolones, cases of hyperglycemia and hypoglycemia have been reported with levofloxacin. During levofloxacin therapy, dysglycemia was more likely to occur in elderly patients and patients with diabetes mellitus receiving concomitant therapy with oral hypoglycemic drugs (for example, glibenclamide) or insulin. When using levofloxacin, such patients are at risk of developing hypoglycemia, up to hypoglycemic coma. It is necessary to inform patients about the symptoms of hypoglycemia (confusion, dizziness, “wolfish” appetite, headache, nervousness, palpitation or rapid pulse, pallor of the skin, perspiration, trembling, weakness). If the patient develops hypoglycemia, it is necessary to immediately stop treatment with levofloxacin and start appropriate therapy. In these cases, it is recommended to switch to therapy with an antibiotic other than fluoroquinolones, if possible. When conducting treatment with levofloxacin in elderly patients, in patients with diabetes mellitus, careful monitoring of blood glucose concentration is recommended.

Peripheral neuropathy

Patients taking fluoroquinolones, including levofloxacin, have been reported to develop sensory and sensorimotor peripheral neuropathy, the onset of which may be rapid. If the patient develops symptoms of neuropathy, levofloxacin should be discontinued. This minimizes the possible risk of irreversible changes.

Patients should be informed about the need to inform their attending physician about any symptoms of neuropathy. Fluoroquinolones should not be used in patients with a history of peripheral neuropathy.

Exacerbation of pseudoparalytic myasthenia gravis

Fluoroquinolones, including levofloxacin, are characterized by neuromuscular blocking activity and may increase muscle weakness in patients with pseudoparalytic myasthenia gravis. Adverse reactions have been reported, including pulmonary insufficiency that required mechanical ventilation and death, which have been associated with the use of fluoroquinolones in patients with pseudoparalytic myasthenia gravis. The use of levofloxacin in patients with an established diagnosis of pseudoparalytic myasthenia gravis is not recommended (see the section “Side effects”).

Psychotic reactions

Psychotic reactions, including suicidal thoughts/attempts, have been reported in patients taking fluoroquinolones, including levofloxacin, sometimes after a single dose. In case of any side effects from the central nervous system, including mental disorders, treatment with levofloxacin should be stopped immediately and appropriate therapy should be prescribed. In these cases, it is recommended to switch to therapy with an antibiotic other than fluoroquinolones, if possible. Caution should be exercised when prescribing the drug to patients with psychosis or a history of mental illness.

Visual disturbances

If you develop any visual disturbances, you should immediately consult an ophthalmologist (see the section “Side effects”).

Impact on laboratory tests

In patients taking levofloxacin, the determination of opiates in the urine may lead to false positive results, which should be confirmed by more specific methods.

Levofloxacin can inhibit the growth of Mycobacterium tuberculosis and subsequently lead to false negative results of the bacteriological diagnosis of tuberculosis.

Influence on the ability to drive vehicles and mechanisms

Side effects of levofloxacin such as dizziness or vertigo, drowsiness, and visual disturbances may reduce psychomotor responses and the ability to concentrate. During the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

At a temperature not exceeding 25°C.

Keep out of reach of children.

Shelf

life is 3 years.

Do not use after the expiration date.

Active ingredient

Levofloxacin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets