Levofloxacin-Vertex, 250 mg 10 pcs

Pharmacotherapeutic group:

An antimicrobial agent, fluoroquinolone.

ATC code:

[J01MA12].

Pharmacological properties

Pharmacodynamics

Levofloxacin is a synthetic broad-spectrum antibacterial drug from the group of fluoroquinolones, probably as the active substance levofloxacin – the left-handed isomer ofloxacin.

Levofloxacin blocks DNA-giase, causes superspiralization and cross-linking of DNA breaks, inhibits DNA synthesis and causes morphological changes in cytoplasm, cell wall and membranes.

Levofloxacin is active against most strains under in vitro as well as in vivo conditions. Aerobic Gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus faecalis, Enterococcus spp, Listeria monocytogenes, Staphylococcus coagulazonegative 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/Ampi-R ducreyi, Haemophilus influenza. Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella oxytoca, Klebsiella pneumoniae, Klebsiella spp, Moraxela catarrhalis β+/β-, Morganella morganii, Neisseria gonorrhoeae non PPNG/PPNG, Neisseria meningitidis, Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida, Pasteurella mirabili, Proteus mirabili , Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Providencia species, Pseudomonas aeruginosa, Pseudomonas species, Salmonella species, Serratia marcescens species, Serratia species.

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. Veilonella species.

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. Veilonella species. 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 quickly and almost completely absorbed after oral administration. Low rate ingestion and complete absorption. The bioavailability of 500 mg of levofloxacin after oral administration is almost 100%.

After a single dose of 500 mg of levofloxacin the concentration is 5.2-6.9 mcg/ml, the time to reach the expected result is 1.3 h, the elimination half-life is 6-8 h. Binding with plasma proteins is 30-40%. It penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, urogenital organs, bone tissue, cerebrospinal fluid, prostate, polymorphonuclear leukocytes, alveolar macrophages.

In the liver, a small portion is oxidized and/or deacetylated. It is excreted from natural dependence by glomerular filtration and tubular secretion.

Indications

Infectious inflammatory diseases caused by susceptible microorganisms:

Active ingredient

Composition

1 film-coated tablet contains:

Active substance:

levofloxacin hemihydrate 256.23 mg, which corresponds to the content of levofloxacin – 250 mg, (in terms of levofloxacin hemihydrate – 256.23 mg).

Auxiliary substances:

Microcrystalline cellulose,

Hypromellose (hydroxypropyl methylcellulose),

Primellose (croscarmellose sodium),

calcium stearate.

Composition of the shell:

hypromellose,

macrogol 4000,

talc,

How to take, the dosage

The drug is taken orally 1 or 2 times a day. Tablets should not be chewed and should be swallowed with enough liquid (0.5 to 1 cup), it can be taken 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.

Patients with normal or moderately reduced renal function (creatinine clearance > 50 ml/min) are recommended the following dosing regimen of the drug: sinusitis: 500 mg once daily – 10-14 days; exacerbation of chronic bronchitis: 250 mg or 500 mg once daily – 7-10 days; community-acquired pneumonia: 500 mg 1-2 times daily – 7-14 days.

Uncomplicated urinary tract infections: 250 mg once daily for 3 days; prostatitis: 500 mg once daily for 28 days; complicated urinary tract infections, including pyelonephritis: 250 mg once daily for 7-10 days; skin and soft tissue infections:250 mg once daily or 500 mg 1-2 times daily – 7-14 days; septicemia/bacteremia: 250 mg or 500 mg 1-2 times daily – 10-14 days; intraabdominal infection: 250 mg or 500 mg once daily – 7-14 days (in combination with antibacterials acting on anaerobic flora).

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

Patients with impaired liver function do not require special dosing because levofloxacin is only very slightly metabolized in the liver.

As with 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.

Interaction

The combined use of Levofloxacin with Phenbufen, nonsteroidal anti-inflammatory drugs (e.g., Aspirin, Paracetamol, Ibuprofen, Nimesulide, etc.) and theophylline increases the CNS readiness for seizures.

The efficacy of Levofloxacin is reduced when concomitant use with Sucralfate, antacids (e.g. Almagel, Renia, Fosfalugel, etc.) and iron salts. In order to offset the effect of the listed drugs on Levofloxacin, it is necessary to separate their intake by 2 hours.

The combined use of Levofloxacin and glucocorticoids (e.g., hydrocortisone, prednisolone, Methylprednisolone, dexamethasone, betamethasone, etc.) leads to an increased risk of tendon rupture.

The intake of alcoholic beverages together with Levofloxacin leads to increased CNS side effects (dizziness, somnolence, visual impairment, loss of concentration and poor response).

Special Instructions

Levofloxacin should not be used in children and adolescents because of the possibility of damage to articular cartilage.

When treating elderly patients it should be borne in mind that patients in this group often have impaired renal function (see section “Dosage and administration”).

In severe pneumococcal pneumonia, levofloxacin may not have optimal therapeutic effect. Hospital infections caused by certain pathogens (P. aeruginosa) may require combination therapy.

When treated with Levofloxacin, seizures may develop in patients with prior brain damage due to, for example, stroke or severe trauma.

While photosensitization is very rare with levofloxacin, patients should avoid unnecessary exposure to strong sunlight or artificial ultraviolet radiation to avoid this.

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

Tendinitis (primarily inflammation of the Achilles tendon) that is rarely observed with the use of Levofloxacin may lead to tendon rupture. Older patients are more prone to tendinitis. Treatment with glucocorticosteroids is likely to increase the risk of tendon rupture. If tendinitis 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 (hereditary metabolic disorder) may respond to fluoroquinolones by destruction of red blood cells (hemolysis). In this regard, treatment of such patients with levofloxacin should be performed with great caution.

Impact on driving and operating machinery

Such side effects of Levofloxacin as dizziness or stupor, somnolence and visual disturbances (see also section “Side effects”) may impair the ability to react and concentrate. This may pose some risk in situations where these abilities are particularly important (e.g., driving, operating machinery and equipment, or working in unsteady positions).

Contraindications

Side effects

Classification of the frequency of side effects according to the recommendations of the World Health Organization (WHO): very often >1/10; often from >1/100 to <1/10; infrequent from >1/1000 to <1/100; rare from >1/10000 to <1/1000; very rare <1/10000, including individual reports; frequency unknown – based on available data it is impossible to determine the incidence.

Cardiac disorders: rare – sinus tachycardia, palpitations; frequency is unknown – prolongation of QT interval, ventricular pirouette type tachycardia that may lead to cardiac arrest (See sections “Overdose” and “Special Indications”).

Blood and lymphatic system disorders: infrequent – leukopenia, eosinophilia, rarely – neutropenia, thrombocytopenia; frequency is unknown – pancytopenia, agranulocytosis, hemolytic anemia.

Nervous system disorders: frequently – headache, dizziness; infrequently – somnolence, tremor, dysgeusia (perversion of taste); rarely – paresthesia and seizures (see section “Indications. Rarely – paresthesia, seizures (see section “Special Indications”); frequency unknown – peripheral sensory neuropathy, peripheral sensorimotor neuropathy, dyskinesia, extrapyramidal disorders, aguesia (loss of sense of taste), parosmia (disorder of sense of smell, especially subjective smell sense, objectively absent), including sense of smell loss, syncope, benign intracranial hypertension.

Visual disorders: very rare – visual disturbances such as blurred vision; frequency is unknown – transient loss of vision.

Hearing and labyrinth disorders: infrequent – vertigo (feeling of deviation or spinning or own body or surrounding objects); rare – tinnitus; frequency unknown – decreased hearing, hearing loss.

Respiratory system, chest and mediastinum disorders: infrequent – shortness of breath; frequency unknown – bronchospasm, allergic pneumonitis.

Gastrointestinal disorders: frequently – diarrhea, vomiting, nausea, infrequently – abdominal pain, dyspepsia, flatulence, constipation; frequency is unknown – hemorrhagic diarrhea which in very rare cases may be a sign of enterocolitis, including pseudomembranous colitis) (see section “Indications”), pancreatitis.

Renal and urinary tract disorders: infrequent – increase in plasma creatinine concentration; rarely – acute renal failure (e.g., due to interstitial nephritis).

Skin and subcutaneous tissue disorders: infrequent – rash, pruritus, urticaria, hyperhidrosis; frequency is unknown – toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema exudative multiforme, photosensitization reactions (see sect.

Skin and mucous membranes side effects may sometimes develop even after the first dose of the drug.

Musculoskeletal and connective tissue disorders: infrequent – arthralgia, myalgia; rare – tendon disorders, including tendinitis, muscle weakness that may be especially dangerous in patients with myasthenia gravis (see sect.

Specific information); frequency is unknown – rhabdomyolysis, tendon rupture (this side effect may be observed within 48 hours after treatment initiation and may be bilateral), ligament tears, muscle tears, arthritis.

Metabolic and nutritional disorders: infrequent – anorexia; rare – hypoglycemia, especially in patients with diabetes (possible signs of hypoglycemia: “wolf” appetite, nervousness, sweating, trembling); frequency is unknown – hyperglycemia, hypoglycemic coma (see section “Indications”).

Infectious and parasitic diseases: infrequent – fungal infections, development of resistance of pathogens.

Vascular disorders: rare – decreased blood pressure;

General disorders: infrequent – asthenia; rare – pyrexia; frequency unknown – pain (including pain in the back, chest and extremities).

Immune system disorders: rare – angioedema; frequency unknown – anaphylactic shock, anaphylactoid shock.

Anaphylactic and anaphylactoid reactions may sometimes develop even after the first dose of the drug.

Disorders of the liver and biliary tract: frequent – increased activity of “liver” enzymes, increased activity of alkaline phosphatase and gamma-glutamyltransferase; infrequent – increased concentration of bilirubin in blood plasma; frequency unknown – severe liver failure, including cases of acute liver failure, sometimes with fatal outcome, especially in patients with severe underlying disease (such as patients with sepsis), hepatitis, jaundice.

Mental disorders: frequently – insomnia; infrequently – anxiety, anxiety, confusion; rarely – mental disorders (e.g., hallucinations, paranoia), depression, agitation (agitation), sleep disorders, nightmares; frequency is unknown – mental disorders with behavioral disorders with self-harm, including suicidal thoughts and suicide attempts.

Other possible side effects relevant to all fluoroquinolones: very rare – exacerbation of porphyria.

Overdose

Symptoms of Levofloxacin overdose are manifested at CNS level (confusion, dizziness, impaired consciousness and seizure-like epileptic seizures). Gastrointestinal disorders (e.g., nausea) and mucosal erosions, prolongation of the Q-T interval may also be noted.

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

Similarities