Possibilities of clinical use of levofloxacin

Composition and release form

Tablets - 1 tablet:

• Active ingredients: levofloxacin hemihydrate - 512.46 mg (corresponding to the content of levofloxacin - 500 mg);
• Excipients: microcrystalline cellulose - 44.69 mg, crospovidone - 7.85 mg, sodium stearyl fumarate - 1.41 mg, croscarmellose sodium - 6.15 mg, colloidal silicon dioxide - 15.38 mg, maltodextrin - 24.6 mg, magnesium stearate - 2.46 mg;
• Shell composition: Opadry orange 20A230018 - 15 mg (hydroxypropyl methylcellulose 2910 [hypromellose 6cP] (E464) - 6.6 mg, titanium dioxide (E171) - 1.375 mg, talc - 3.150 mg, hyprolose [hydroxypropylcellulose, klucel EF] ( E463) - 3.851 mg, sunset yellow dye (E110) - 0.024 mg).

3/5/7/10 pcs. — contour packaging, cardboard packs.

Composition per tablet:

Description of the dosage form

Film-coated tablets, pinkish-orange, oval, biconvex; When cut, it is white to light yellow in color.

pharmachologic effect

Levofloxacin is a synthetic broad-spectrum antibacterial drug from the group of fluoroquinolones, containing levofloxacin, a 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.

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

Aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus faecalis, Enterococcus spp, Listeria monocytogenes, Staphylococcus coagulase-negative methi-S(I), Staphylococcus aureus methi-S, Staphylococcus epidermidis methi-S, Staphylococcus spp(CNS), Streptococci group C and G, Streptococcus agalactiae, Streptococcus pneumoniae peni I/S/R, Streptococcus pyogenes, Viridans streptococci peni-S/R.

Aerobic gram-negative microorganisms: Acinetobacter baumannil, Acinetobacter spp, Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Enterobacter spp, Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae ampi-S/R, Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella oxytoca, Klebsiella pneumoniae, Klebsiella spp, Moraxela catarrhalis (3+/p-, Morganella morganii, Neisseria gonorrhoeae non PPNG/PPNG, Neisseria meningitidis, Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida, Pasteurella spp, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Providencia spp, Pseudomonas aeruginosa, Pseudomonas spp, Salmonella spp, Serratia marcescens, Serratia spp.

Anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp, Clostridium perfringens, Fusobacterium spp, Peptostreptococcus, Propionibacterum spp, Veilonella spp.

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

Pharmacokinetics

Levofloxacin is rapidly and almost completely absorbed after oral administration. Food intake has little effect on the speed and completeness of absorption. The bioavailability of 500 mg levofloxacin after oral administration is almost 100%. After taking a single dose of 500 mg of levofloxacin, Cmax is 5.2-6.9 mcg/ml, the time to reach Cmax is 1.3 hours, T1/2 is 6-8 hours.

Bonding with plasma proteins is 30-40%. Penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, genitourinary organs, bone tissue, cerebrospinal fluid, prostate gland, polymorphonuclear leukocytes, alveolar macrophages.

In the liver, a small portion is oxidized and/or deacetylated. It is excreted from the body primarily by the kidneys by glomerular filtration and tubular secretion. After oral administration, approximately 87% of the dose taken is excreted unchanged in the urine within 48 hours, less than 4% in the feces within 72 hours.

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. Levofloxacin is considered stronger than its substitute, especially when treating coronavirus.

Indications for use of Levofloxacin

Infectious and inflammatory diseases caused by sensitive microorganisms:

• acute sinusitis;
• exacerbation of chronic bronchitis;
• community-acquired pneumonia;
• complicated urinary tract infections (including pyelonephritis);
• uncomplicated urinary tract infections;
• prostatitis;
• infections of the skin and soft tissues;
• septicemia/bacteremia associated with the above indications;
• intra-abdominal infection.

Levofloxacin or Amoxiclav - which is better for pneumonia

Manufacturer: SANDOS, Slovenia
Release form: powder for suspensions, tablets

Active ingredient: amoxicillin + clavulanic acid

Amoxiclav is an analogue cheaper than Levofloxacin. This is an antimicrobial agent with a wide spectrum of action, which is prescribed to patients for various infectious diseases in gynecology, otolaryngology, urology, and pulmonology. It is prescribed to children from birth, but depending on the form of release. The antibiotic contains a penicillin series of substances. Has a detrimental effect on organisms and strains that are not resistant to amoxicillin.

Indications for taking the imported analogue do not depend on the patient’s age group. This substitute for Levofloxacin 500 mg is prescribed for the following infectious diseases and disorders:

1. Upper respiratory tract and ENT organs.
2. Lower respiratory tract.
3. Urinary tract and genital organs.
4. Skin, soft tissues.
5. Bone and connective tissue.
6. Biliary tract.
7. For odontogenic infections.

For pneumonia, it is recommended to use one of the drugs presented, since they are effective for this disorder and can stabilize the patient’s condition within several days.

Contraindications to the use of Levofloxacin

• hypersensitivity to levofloxacin or other quinolones;
• renal failure (with creatinine clearance less than 20 ml/min. - due to the impossibility of dosing this dosage form);
• epilepsy;
• tendon lesions due to previous treatment with quinolones;
• childhood and adolescence (up to 18 years);
• pregnancy and lactation period.

It should be used with caution in the elderly due to the high likelihood of a concomitant decrease in renal function, as well as in cases of glucose-6-phosphate dehydrogenase deficiency.

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").

Use of Levofloxacin during pregnancy and children

The incidence of levofloxacin-related adverse reactions in Phase 3 clinical trials conducted in North America was 6.3%. Therapy was discontinued due to drug-related side effects in 3.9% of patients.

In clinical studies, the following side effects were considered likely to be related to levofloxacin: nausea (1.3%), diarrhea (1%), vaginitis (0.7%), insomnia (0.5%), abdominal pain (0. 4%), flatulence (0.4%), itching (0.4%), dizziness (0.3%), dyspepsia (0.3%), rash (0.3%), genital candidiasis (0. 2%), taste disturbance (0.2%), vomiting (0.2%), constipation (0.1%), fungal infection (0.1%), itching in the genital area (0.1%), headache pain (0.1%), thrush (0.1%), nervousness (0.1%), erythematous rash (0.1%), urticaria (0.1%).

In clinical studies, the following side effects were observed without taking into account the relationship with the drug.

From the nervous system and sensory organs: headache (6.4%), insomnia (4.6%), dizziness (2.7%), fatigue (1.2%), impaired taste sensitivity (1%); <1%: asthenia, incoordination, coma, convulsions, speech impairment, stupor, tremor, vertigo, confusion, aggression, agitation, anxiety, anorexia, delirium, depression, emotional lability, hallucinations, difficulty concentrating, mania, nervousness, paranoia, impaired thinking, unusual dreams, sleep disturbance, somnolence, diplopia, cerebrovascular disorders, tinnitus, hearing and vision impairment, conjunctivitis, parosmia.

From the cardiovascular system and blood <1%: hypertension, hypotension (including orthostatic), heart failure, circulatory failure, arrhythmia, bradycardia, tachycardia, blockade, cardiac arrest, supraventricular tachycardia, ventricular and atrial fibrillation, palpitation , angina pectoris, coronary thrombosis, myocardial infarction, thromboembolism, phlebitis, platelet pathology, epistaxis, purpura, thrombocytopenia, leukocytosis, leukopenia, lymphopenia, granulocytopenia, lymphadenopathy.

From the respiratory system: sinusitis (1.3%), rhinitis (1%); <1%: asthma, acute respiratory distress syndrome, cough, hemoptysis, dyspnea, hypoxia, pleural effusion, respiratory failure.

From the gastrointestinal tract: nausea (7.2%), diarrhea (5.6%), constipation (3.2%), abdominal pain (2.5%), dyspepsia (2.4%), vomiting (2 .3%), flatulence (1.5%); <1%: dry mouth, dysphagia, swelling of the tongue, gastroenteritis, gastrointestinal bleeding, pseudomembranous colitis, hepatic coma, increased LDH, jaundice, impaired liver function, cholelithiasis.

From the genitourinary system: vaginitis (1.8%); <1%: itching in the genital area, impaired ejaculation, impotence, increased serum creatinine, decreased renal function, acute renal failure, hematuria.

From the musculoskeletal system <1%: arthralgia, arthritis, arthrosis, muscle weakness, myalgia, osteomyelitis, synovitis, tendonitis, rhabdomyolysis, hyperkinesis, involuntary muscle contractions, increased muscle tone, paresthesia, paralysis.

From the skin: itching (1.3%), rash (1.2%); <1%: erythema nodosum, skin peeling, skin ulceration, urticaria, increased sweating.

Other: local reaction (3.5%), pain (1.7%) and inflammation (1.1%) at the injection site; pain (1.4%), chest pain (1.2%) and back pain (1.1%); <1%: hyperkalemia, hypokalemia, dehydration, hypoglycemia, hyperglycemia, worsening diabetes mellitus, weight loss, carcinoma, fever, facial edema, withdrawal syndrome.

The following adverse effects have been reported in post-marketing studies: hypersensitivity pneumonitis, anaphylactic shock, anaphylactoid reaction, dysphonia, abnormal EEG, encephalopathy, eosinophilia, erythema multiforme, hemolytic anemia, multiple organ failure, increased international normalized ratio (INR), Stevens-Johnson syndrome, rupture tendons, ventricular fibrillation, vasodilation.

Below are data from 29 pooled Phase 3 clinical trials (n=7537). The average age of patients is 50 years (approximately 74% of patients are younger than 65 years), 50% are male, 71% are Caucasian, and 19% are black. Patients received levofloxacin for the treatment of various infections at a dose of 750 mg once daily, 250 mg once daily, or 500 mg twice daily. The duration of therapy was usually 3–14 days (average 10 days).

The overall incidence, type, and distribution of adverse reactions were similar in patients receiving levofloxacin 750 mg once daily compared with patients receiving 250 mg once daily or 500 mg twice daily. Therapy was discontinued due to drug-related adverse events in 4.3% of patients overall, 3.8% of patients taking the 250 and 500 mg doses, and 5.4% of patients taking the 750 mg dose. The most common side effects leading to discontinuation of the drug at doses of 250 and 500 mg were gastrointestinal complaints (1.4%), nausea (0.6%), vomiting (0.4%), dizziness (0.3%) , headache (0.2%). The most common side effects leading to discontinuation of the drug at a dose of 750 mg were gastrointestinal disturbances (1.2%), nausea (0.6%), vomiting (0.5%), dizziness (0.3%), headache pain (0.3%).

The following are side effects noted in clinical trials and observed with an incidence of more than 0.1%.

From the nervous system and sensory organs: headache (6%), dizziness (3%), insomnia (4%); 0.1–1%: anxiety, agitation, confusion, depression, hallucinations, nightmares, sleep disturbances, anorexia, unusual dreams, tremors, convulsions, paresthesia, vertigo, hypertension, hyperkinesis, incoordination, drowsiness, fainting.

From the cardiovascular system and blood: 0.1–1%: anemia, arrhythmia, palpitations, cardiac arrest, supraventricular tachycardia, phlebitis, epistaxis, thrombocytopenia, granulocytopenia.

From the respiratory system: shortness of breath (1%).

From the gastrointestinal tract: nausea (7%), diarrhea (5%), constipation (3%), abdominal pain (2%), dyspepsia (2%), vomiting (2%); 0.1–1%: gastritis, stomatitis, pancreatitis, esophagitis, gastroenteritis, glossitis, pseudomembranous colitis, liver dysfunction, increased levels of liver enzymes, increased alkaline phosphatase.

From the genitourinary system: vaginitis (1%); 0.1–1%: impaired renal function, acute renal failure, genital candidiasis.

From the musculoskeletal system: 0.1–1%: arthralgia, tendinitis, myalgia, skeletal muscle pain.

From the skin: rash (2%), itching (1%); 0.1–1%: allergic reactions, edema (1%), urticaria.

Other: candidiasis (1%), reaction at the IV injection site (1%), chest pain (1%); 0.1–1%: hypoglycemia/hyperglycemia, hyperkalemia.

The following side effects have been reported in post-marketing studies.

From the nervous system and sensory organs: isolated reports of encephalopathy, EEG abnormalities, peripheral neuropathy, psychosis, paranoia, isolated reports of suicide attempts and suicidal thoughts, visual impairment (including diplopia, decreased visual acuity, blurred vision, scotoma ), hearing loss, tinnitus, parosmia, anosmia, loss of taste, taste perversion, dysphonia.

From the cardiovascular system and blood: isolated reports of torsade de pointes, prolongation of the QT interval, tachycardia, vasodilation, increased INR, prolongation of prothrombin time, pancytopenia, aplastic anemia, leukopenia, hemolytic anemia, eosinophilia.

From the gastrointestinal tract: liver failure (including fatal cases), hepatitis, jaundice.

From the musculoskeletal system: tendon rupture, muscle damage, including rupture, rhabdomyolysis.

From the skin: bullous rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, photosensitivity/phototoxicity reactions.

Allergic reactions: hypersensitivity reactions (sometimes fatal), incl. anaphylactic/anaphylactoid reactions, anaphylactic shock, angioedema, serum sickness; isolated reports of hypersensitivity pneumonitis.

Other: vasculitis, increased activity of muscle enzymes, hyperthermia, multiorgan failure, interstitial nephritis.

When using levofloxacin in the form of 0.5% eye drops, the most frequently observed effects were: 1-3% - transient decreased vision, transient burning, pain or discomfort in the eye, sensation of a foreign body in the eye, fever, headache, pharyngitis, photophobia; <1% - allergic reactions, swelling of the eyelids, dry eyes, itching in the eye.

Side effects of Levofloxacin

Allergic reactions: sometimes – itching and redness of the skin; rarely - general hypersensitivity reactions (anaphylactic and anaphylactoid reactions) with symptoms such as urticaria, constriction of the bronchi and possibly severe suffocation; very rarely - swelling of the skin and mucous membranes (for example, in the face and throat), sudden drop in blood pressure and shock, increased sensitivity to solar and ultraviolet radiation, allergic pneumonitis, vasculitis; in some cases - severe skin rashes with blistering, for example, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome) and exudative erythema multiforme. General hypersensitivity reactions may sometimes be preceded by milder skin reactions. The above reactions can develop after the first dose, a few minutes or hours after administration of the drug.

From the digestive system: often - nausea, diarrhea, increased activity of liver enzymes (for example, alanine aminotransferase and aspartate aminotransferase); sometimes - loss of appetite, vomiting, abdominal pain, digestive disorders; rarely - diarrhea mixed with blood, which in very rare cases can be a sign of intestinal inflammation and even pseudomembranous colitis.

On the metabolic side: very rarely - a decrease in the concentration of glucose in the blood, which is of particular importance for patients with diabetes (possible signs of hypoglycemia: increased appetite, nervousness, perspiration, trembling). Experience with the use of other quinolones suggests that they can cause exacerbation of porphyria in patients already suffering from this disease. A similar effect cannot be excluded when using the drug levofloxacin.

From the nervous system: sometimes - headache, dizziness and/or stupor, drowsiness, sleep disturbances; rarely - anxiety, paresthesia in the hands, trembling, psychotic reactions such as hallucinations and depression, agitation, convulsions and confusion; very rarely - impaired vision and hearing, impaired taste and smell, decreased tactile sensitivity.

From the cardiovascular system: rarely - increased heartbeat, decreased blood pressure; very rarely - vascular (shock-like) collapse; in some cases - prolongation of the QT interval.

From the musculoskeletal system: rarely - tendon damage (including tendinitis), joint and muscle pain; very rarely - tendon rupture (for example, Achilles tendon); this side effect can be observed within 48 hours after the start of treatment and can be bilateral in nature, muscle weakness, which is of particular importance for patients with bulbar syndrome; in some cases - muscle damage (rhabdomyolysis).

From the urinary system: rarely - increased levels of bilirubin and creatinine in the blood serum; very rarely - deterioration of kidney function up to acute renal failure, interstitial nephritis.

From the hematopoietic organs: sometimes - an increase in the number of eosinophils, a decrease in the number of leukocytes; rarely - neutropenia, thrombocytopenia, which may be accompanied by increased bleeding; very rarely - agranulocytosis and the development of severe infections (persistent or recurrent increase in body temperature, deterioration in health); in some cases - hemolytic anemia; pancytopenia.

Other: sometimes - general weakness; very rarely - fever.

Any antibiotic therapy can cause changes in the microflora that is normally present in humans. For this reason, increased proliferation of bacteria and fungi resistant to the antibiotic used may occur, which in rare cases may require additional treatment.

Levofloxacin 250 mg 5 pcs. film-coated tablets

pharmachologic effect

Levofloxacin is a synthetic broad-spectrum antibacterial drug from the group of fluoroquinolones, containing levofloxacin, a 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. Levofloxacin is active against most strains of microorganisms both in vitro and in vivo.

Aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus faecalis, Enterococcus spp, Listeria monocytogenes, Staphylococcus coagulase-negative methi-S(I), Staphylococcus aureus methi-S, Staphylococcus epidermidis methi-S, Staphylococcus spp(CNS), Streptococci group C and G, Streptococcus agalactiae, Streptococcus pneumoniae peni I/S/R, Streptococcus pyogenes, Viridans streptococci peni-S/R.

Aerobic gram-negative microorganisms: Acinetobacter baumannil, Acinetobacter spp, Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Enterobacter spp, Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae ampi-S/R, Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella oxytoca, Klebsiella pneumoniae, Klebsiella spp, Moraxela catarrhalis (3+/p-, Morganella morganii, Neisseria gonorrhoeae non PPNG/PPNG, Neisseria meningitidis, Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida, Pasteurella spp, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Providencia spp, Pseudomonas aeruginosa, Pseudomonas spp, Salmonella spp, Serratia marcescens, Serratia spp.

Anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp, Clostridium perfringens, Fusobacterium spp, Peptostreptococcus, Propionibacterum spp, Veilonella spp.

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

Composition and release form Levofloxacin 250 mg 5 pcs. film-coated tablets

Tablets - 1 tablet:

• Active ingredients: levofloxacin hemihydrate - 256.23 mg. 9 corresponds to the content of levofloxacin - 250 mg);
• Excipients: microcrystalline cellulose, hypromellose (hydroxypropyl methylcellulose), primellose (croscarmellose sodium), calcium stearate.
• Shell composition: hypromellose, macrogol 4000, talc, titanium dioxide, yellow iron oxide dye.

5/10 pcs. — polymer cans/blister packaging, cardboard packs.

Description of the dosage form

Yellow film-coated tablets, round, biconvex; On a cross section, two layers are visible.

Directions for use and doses

The drug is taken orally 1 or 2 times a day. Do not chew the tablets and take a sufficient amount of liquid (from 0.5 to 1 glass); you can take them before meals or between meals. Doses are determined by the nature and severity of the infection, as well as the sensitivity of the suspected pathogen.

For patients with normal or moderately reduced renal function (creatinine clearance > 50 ml/min.), the following dosage regimen is recommended: sinusitis: 500 mg 1 time per day - 10-14 days; exacerbation of chronic bronchitis: 250 mg or 500 mg 1 time per day - 7-10 days; community-acquired pneumonia: 500 mg 1-2 times a day - 7-14 days. uncomplicated urinary tract infections: 250 mg 1 time per day for 3 days; prostatitis: 500 mg - 1 time per day - 28 days; complicated urinary tract infections, including pyelonephritis: 250 mg 1 time per day - 7-10 days; infections of the skin and soft tissues: 250 mg 1 time a day or 500 mg 1-2 times a day - 7-14 days; septicemia/bacteremia: 250 mg or 500 mg 1-2 times a day for 10-14 days; intra-abdominal infection: 250 mg or 500 mg 1 time per day - 7-14 days (in combination with antibacterial drugs acting on anaerobic flora).

Patients undergoing hemodialysis or continuous ambulatory peritoneal dialysis do not require additional doses.

Patients with impaired liver function do not require special dosing, since levofloxacin is metabolized in the liver only to an extremely small extent.

As with the use of other antibiotics, treatment with Levofloxacin is recommended to be continued for at least 48-78 hours after normalization of body temperature or after laboratory confirmed recovery.

Pharmacokinetics

Levofloxacin is rapidly and almost completely absorbed after oral administration. Food intake has little effect on the speed and completeness of absorption. The bioavailability of 500 mg levofloxacin after oral administration is almost 100%. After taking a single dose of 500 mg of levofloxacin, Cmax is 5.2-6.9 mcg/ml, the time to reach Cmax is 1.3 hours, T1/2 is 6-8 hours.

Bonding with plasma proteins is 30-40%. Penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, genitourinary organs, bone tissue, cerebrospinal fluid, prostate gland, polymorphonuclear leukocytes, alveolar macrophages.

In the liver, a small portion is oxidized and/or deacetylated. It is excreted from the body primarily by the kidneys by glomerular filtration and tubular secretion. After oral administration, approximately 87% of the dose taken is excreted unchanged in the urine within 48 hours, less than 4% in the feces within 72 hours.

Indications for use Levofloxacin 250 mg 5 pcs. film-coated tablets

Infectious and inflammatory diseases caused by sensitive microorganisms:

• acute sinusitis;
• exacerbation of chronic bronchitis;
• community-acquired pneumonia;
• complicated urinary tract infections (including pyelonephritis);
• uncomplicated urinary tract infections;
• prostatitis;
• infections of the skin and soft tissues;
• septicemia/bacteremia associated with the above indications;
• intra-abdominal infection.

Contraindications

• hypersensitivity to levofloxacin or other quinolones;
• renal failure (with creatinine clearance less than 20 ml/min. - due to the impossibility of dosing this dosage form);
• epilepsy;
• tendon lesions due to previous treatment with quinolones;
• childhood and adolescence (up to 18 years);
• pregnancy and lactation period.

It should be used with caution in the elderly due to the high likelihood of a concomitant decrease in renal function, as well as in cases of glucose-6-phosphate dehydrogenase deficiency.

Application Levofloxacin 250 mg 5 pcs. film-coated tablets during pregnancy and breastfeeding

Contraindicated during pregnancy and lactation. Levofloxacin should not be used to treat children and adolescents (under 18 years of age) due to the likelihood of damage to articular cartilage.

special instructions

Levofloxacin should not be used to treat children and adolescents due to the likelihood of damage to articular cartilage.

When treating elderly patients, it should be borne in mind that patients in this group often suffer from impaired renal function.

In severe pneumonia caused by pneumococci, levofloxacin may not provide an optimal therapeutic effect. Hospital-acquired infections caused by certain pathogens (P. aeruginosa) may require combination treatment.

During treatment with Levofloxacin, seizures may develop in patients with previous brain damage caused, for example, by stroke or severe trauma.

Despite the fact that photosensitivity is observed very rarely with the use of levofloxacin, in order to avoid it, patients are not recommended to be exposed to strong solar or artificial ultraviolet irradiation unnecessarily.

If pseudomembranous colitis is suspected, levofloxacin should be discontinued immediately and appropriate treatment should be initiated. In such cases, drugs that inhibit intestinal motility should not be used.

Rarely observed with the use of the drug Levofloxacin, tendonitis (primarily inflammation of the Achilles tendon) can lead to tendon rupture. Elderly patients are more prone to tendinitis. Treatment with glucocorticosteroids appears to increase the risk of tendon rupture. If tendonitis is suspected, treatment with Levofloxacin should be stopped immediately and appropriate treatment of the affected tendon should be initiated.

Patients with glucose-6-phosphate dehydrogenase deficiency (an inherited metabolic disorder) may respond to fluoroquinolones by destroying red blood cells (hemolysis). In this regard, treatment of such patients with levofloxacin should be carried out with great caution.

Impact on the ability to drive vehicles and operate machinery

Side effects of Levofloxacin, such as dizziness or drowsiness, drowsiness and visual disturbances, may impair reactivity and ability to concentrate. This may pose a risk in situations where these abilities are of particular importance (for example, when driving a car, when servicing machinery, when performing work in an unstable position).

Overdose

Symptoms of an overdose of Levofloxacin appear at the level of the central nervous system (confusion, dizziness, disturbances of consciousness and seizures of the epileptic type). In addition, gastrointestinal disorders (for example, nausea) and erosive lesions of the mucous membranes, prolongation of the QT interval may occur.

Treatment should be symptomatic. Levofloxacin is not eliminated by dialysis (hemodialysis, peritoneal dialysis and continuous peritoneal dialysis). There is no specific antidote.

Side effects Levofloxacin 250 mg 5 pcs. film-coated tablets

Allergic reactions: sometimes – itching and redness of the skin; rarely - general hypersensitivity reactions (anaphylactic and anaphylactoid reactions) with symptoms such as urticaria, constriction of the bronchi and possibly severe suffocation; very rarely - swelling of the skin and mucous membranes (for example, in the face and throat), sudden drop in blood pressure and shock, increased sensitivity to solar and ultraviolet radiation, allergic pneumonitis, vasculitis; in some cases - severe skin rashes with blistering, for example, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome) and exudative erythema multiforme. General hypersensitivity reactions may sometimes be preceded by milder skin reactions. The above reactions can develop after the first dose, a few minutes or hours after administration of the drug.

From the digestive system: often - nausea, diarrhea, increased activity of liver enzymes (for example, alanine aminotransferase and aspartate aminotransferase); sometimes - loss of appetite, vomiting, abdominal pain, digestive disorders; rarely - diarrhea mixed with blood, which in very rare cases can be a sign of intestinal inflammation and even pseudomembranous colitis.

On the metabolic side: very rarely - a decrease in the concentration of glucose in the blood, which is of particular importance for patients with diabetes (possible signs of hypoglycemia: increased appetite, nervousness, perspiration, trembling). Experience with the use of other quinolones suggests that they can cause exacerbation of porphyria in patients already suffering from this disease. A similar effect cannot be excluded when using the drug levofloxacin.

From the nervous system: sometimes - headache, dizziness and/or stupor, drowsiness, sleep disturbances; rarely - anxiety, paresthesia in the hands, trembling, psychotic reactions such as hallucinations and depression, agitation, convulsions and confusion; very rarely - impaired vision and hearing, impaired taste and smell, decreased tactile sensitivity.

From the cardiovascular system: rarely - increased heartbeat, decreased blood pressure; very rarely - vascular (shock-like) collapse; in some cases - prolongation of the QT interval.

From the musculoskeletal system: rarely - tendon damage (including tendinitis), joint and muscle pain; very rarely - tendon rupture (for example, Achilles tendon); this side effect can be observed within 48 hours after the start of treatment and can be bilateral in nature, muscle weakness, which is of particular importance for patients with bulbar syndrome; in some cases - muscle damage (rhabdomyolysis).

From the urinary system: rarely - increased levels of bilirubin and creatinine in the blood serum; very rarely - deterioration of kidney function up to acute renal failure, interstitial nephritis.

From the hematopoietic organs: sometimes - an increase in the number of eosinophils, a decrease in the number of leukocytes; rarely - neutropenia, thrombocytopenia, which may be accompanied by increased bleeding; very rarely - agranulocytosis and the development of severe infections (persistent or recurrent increase in body temperature, deterioration in health); in some cases - hemolytic anemia; pancytopenia.

Other: sometimes - general weakness; very rarely - fever.

Any antibiotic therapy can cause changes in the microflora that is normally present in humans. For this reason, increased proliferation of bacteria and fungi resistant to the antibiotic used may occur, which in rare cases may require additional treatment.

Drug interactions

There are reports of a pronounced decrease in the threshold of convulsive readiness with the simultaneous use of quinolones and substances that can, in turn, reduce the cerebral threshold of convulsive readiness. This also applies equally to the simultaneous use of quinolones and theophylline.

The effect of Levofloxacin is significantly weakened when used simultaneously with sucralfate. The same thing happens with the simultaneous use of magnesium or aluminum containing antacids, as well as iron salts. Levofloxacin should be taken at least 2 hours before or 2 hours after taking these medications. No interaction was detected with calcium carbonate.

When using vitamin K antagonists simultaneously, monitoring of the blood coagulation system is necessary.

The elimination (renal clearance) of levofloxacin is slightly slowed down by the action of cimetidine and probenecid. It should be noted that this interaction has virtually no clinical significance. However, with the simultaneous use of drugs such as probenecid and cimetidine, which block a certain excretion pathway (tubular secretion), treatment with levofloxacin should be carried out with caution. This applies primarily to patients with limited renal function.

Levofloxacin slightly increases the half-life of cyclosporine.

Taking glucocorticosteroids increases the risk of tendon rupture.

Drug interactions

There are reports of a pronounced decrease in the threshold of convulsive readiness with the simultaneous use of quinolones and substances that can, in turn, reduce the cerebral threshold of convulsive readiness. This also applies equally to the simultaneous use of quinolones and theophylline.

The effect of Levofloxacin is significantly weakened when used simultaneously with sucralfate. The same thing happens with the simultaneous use of magnesium or aluminum containing antacids, as well as iron salts. Levofloxacin should be taken at least 2 hours before or 2 hours after taking these medications. No interaction was detected with calcium carbonate.

When using vitamin K antagonists simultaneously, monitoring of the blood coagulation system is necessary.

The elimination (renal clearance) of levofloxacin is slightly slowed down by the action of cimetidine and probenecid. It should be noted that this interaction has virtually no clinical significance. However, with the simultaneous use of drugs such as probenecid and cimetidine, which block a certain excretion pathway (tubular secretion), treatment with levofloxacin should be carried out with caution. This applies primarily to patients with limited renal function.

Levofloxacin slightly increases the half-life of cyclosporine.

Taking glucocorticosteroids increases the risk of tendon rupture.

special instructions

Levofloxacin eye drops can only be used topically. The solution cannot be injected into the anterior chamber of the eye or subconjunctivally.

The solution contains benzalkonium chloride, which is a preservative. In this regard, there is no need to use the drug when wearing hydrophilic contact lenses, because in this case eye irritation may occur. If there are signs of bacterial conjunctivitis, then contact methods of refractive correction should be completely abandoned.

Due to the fact that after instillation of the medicine, a temporary decrease in vision may occur, it is not recommended to engage in potentially hazardous activities during this period, in particular, driving a car.

Due to the fact that systemic fluoroquinolols can lead to serious allergic reactions even after a single dose, Levofloxacin eye drops should be discontinued if signs of allergy and hypersensitivity occur.

If you use the drug for a long time, there is a high probability of resistance developing in microorganisms, as well as the growth of fungal flora. If there is a decrease in the effectiveness of Levofloxacin eye drops or an increase in clinical symptoms, then it is necessary to change the medicine to another antibiotic.

Levofloxacin dosage

The drug is taken orally 1 or 2 times a day. Do not chew the tablets and take a sufficient amount of liquid (from 0.5 to 1 glass); you can take them before meals or between meals. Doses are determined by the nature and severity of the infection, as well as the sensitivity of the suspected pathogen.

For patients with normal or moderately reduced renal function (creatinine clearance > 50 ml/min.), the following dosage regimen is recommended: sinusitis: 500 mg 1 time per day - 10-14 days; exacerbation of chronic bronchitis: 250 mg or 500 mg 1 time per day - 7-10 days; community-acquired pneumonia: 500 mg 1-2 times a day - 7-14 days. uncomplicated urinary tract infections: 250 mg 1 time per day for 3 days; prostatitis: 500 mg - 1 time per day - 28 days; complicated urinary tract infections, including pyelonephritis: 250 mg 1 time per day - 7-10 days; infections of the skin and soft tissues: 250 mg 1 time a day or 500 mg 1-2 times a day - 7-14 days; septicemia/bacteremia: 250 mg or 500 mg 1-2 times a day for 10-14 days; intra-abdominal infection: 250 mg or 500 mg 1 time per day - 7-14 days (in combination with antibacterial drugs acting on anaerobic flora).

Patients undergoing hemodialysis or continuous ambulatory peritoneal dialysis do not require additional doses.

Patients with impaired liver function do not require special dosing, since levofloxacin is metabolized in the liver only to an extremely small extent.

As with the use of other antibiotics, treatment with Levofloxacin is recommended to be continued for at least 48-78 hours after normalization of body temperature or after laboratory confirmed recovery.

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.

Overdose

Symptoms of an overdose of Levofloxacin appear at the level of the central nervous system (confusion, dizziness, disturbances of consciousness and seizures of the epileptic type). In addition, gastrointestinal disorders (for example, nausea) and erosive lesions of the mucous membranes, prolongation of the QT interval may occur.

Treatment should be symptomatic. Levofloxacin is not eliminated by dialysis (hemodialysis, peritoneal dialysis and continuous peritoneal dialysis). There is no specific antidote.

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.