Trade name of the drug: Velmex

Active ingredient (INN): levofloxacin

Dosage form: film-coated tablets.

Composition:

1 tablet contains:

active substance: levofloxacin hemihydrate, equivalent to levofloxacin 250 mg, 500 mg or 750 mg;

excipients: corn starch, hydroxypropyl methylcellulose, microcrystalline cellulose, crospovidone, aerosil (silicon dioxide colloidal anhydride), purified talc, magnesium stearate, sodium starch glycollate, sodium croscarmellose, coloring film-coating VINCOO Orange IC14 WT-1416, coloring film coating Wincoat Universal Green WT-3124, coloring film coating Wincoat Universal Green WT-3128

Description:

Velmex 250 mg: light orange to dark orange in color, round, smooth, biconvex film-coated tablet on both sides.

Velmex 500 mg: light green to dark green, elongated, biconvex film-coated tablet with a dividing line on one side.

Velmex 750 mg: light blue to dark blue, elongated, biconvex film-coated tablet with a dividing line on one side.

Pharmacotherapeutic group: Antibacterial synthetic agent (fluoroquinolone group).

ATX code: J01MA12

 

Pharmacological properties

Levofloxacin is a broad-spectrum bactericidal antibiotic from the quinolone group (fluoroquinolone). Levofloxacin is a levorotatory isomer of ofloxacin.
Levofloxacin blocks DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and stitching of DNA breaks, inhibits DNA synthesis, and causes profound morphological changes in the cytoplasm, cell wall and membranes of microorganisms.
Levofloxacin is active against most strains of microorganisms both in vitro and in vivo:

• aerobic gram-positive microorganisms : Corynebacterium diphtheriae; Enterococcus faecalis; Listeria monocytogenes; Staphylococcus spp. (coagulase-negative, methicillin-susceptible / moderate methicillin-susceptible strains), including Staphylococcus aureus, epidermidis (methicillin-susceptible strains); Streptococcus pyogenes, agalactiae, pneumoniae (penicillin-sensitive / moderately penicillin-sensitive / penicillin-resistant strains), Streptococcus (groups C, G), Viridans group streptococci (penicillin-sensitive and penicillin-resistant strains);
• aerobic gram-negative microorganisms : Acinetobacter spp., including Acinetobacter anitratus, baumannii, calcoaceticus; Actinobacillus actinomycetemcomitans; Bordetella pertussis; Citrobacter freundii, diversus; Eikenella corrodens; Enterobacter spp., Including Enterobacter aerogenes, agglomerans, cloacae, sakazakii; Escherichia coli; Gardnerella vaginalis; Haemophilus ducreyi, influenzae ( ampicillinsensitive / ampicillin-resistant strains), Haemophilus parainfluenzae; Helicobacter pylori; Klebsiella spp. Including Klebsiella oxytoca, pneumoniae; Moraxella catarrhalis; Morganella morganii; Neisseria gonorrhoeae (including penicillinase-producing strains), Neisseria meningitidis; Pasteurella spp. Including Pasteurella canis, dagmatis, multocida; Proteus mirabilis, vulgaris; Providencia spp. Including Providencia rettgeri, stuartii; Pseudomonas spp, including Pseudomonas aeruginosa, fluorescens; Salmonella spp .; Serratia spp. Including Serratia marcescens;
• anaerobic microorganisms : Bacteroides fragilis; Bifidobacterium spp .; Clostridium perfringens; Fusobacterium spp .; Peptostreptococcus; Propionibacterium spp .; Veillonella spp .;
• other microorganisms : Bartonella spp .; Chlamydia pneumoniae, psittaci, trachomatis; Legionella spp. Including Legionella pneumophila; Mycobacterium spp., Including Mycobacterium leprae, tuberculosis; Mycoplasma pneumoniae; Rickettsia spp .; Ureaplasma urealyticum.

Pharmacokinetics

After oral administration, levofloxacin is rapidly and almost completely absorbed from the gastrointestinal tract, reaching a maximum concentration in 1-2 hours. Oral bioavailability is about 99%. Protein binding is 24-38%. The drug is well distributed in body tissues. In the lung tissue, the concentration exceeds the plasma concentration by 2-5 times. Levofloxacin undergoes limited metabolism. The half-life of levofloxacin is on average 6-8 hours. After oral administration, approximately 87% of the dose taken is excreted in the urine unchanged within 48 hours, and less than 4% in the feces within 72 hours.

 

Indications for use

Infectious and inflammatory pathology that developed as a result of infection with bacteria sensitive to levofloxacin:

• Abdominal infections
• exacerbation of chronic bronchitis;
• community-acquired form of pneumonia;
• inflammation of the prostate gland;
• acute sinusitis;
• uncomplicated urinary tract infections;
• bacteremia / septicemia (associated with the indications given in the description); • complicated urinary tract infections (including pyelonephritis);
• infectious pathology of soft tissues and skin.

 

Method of administration and dosage

Inside. The drug should be taken whole, without chewing, with plenty of water. Levofloxacin tablets can be taken with or without food. The drug is administered orally to adults as indicated in the table:

 

 

Infection	Dosage	Frequency (times / day)	Duration of treatment (days)
Community-acquired pneumonia	500 mg	one	7-10 days
Community-acquired pneumonia	750 mg	one	5 days
Nosocomial pneumonia	750 mg	one	7-10 days
Complicated skin and soft tissue infections	750 mg	one	7-10 days
Exacerbation of chronic bronchitis	500 mg	one	7 days
Acute sinusitis	500 mg	one	7-10 days
Uncomplicated infections of the skin and subcutaneous fat	500 mg	one	7-10 days
Chronic prostatitis	500 mg	one	10 days
Complicated urinary tract infections	250 mg	one	10 days
Acute pyelonephritis	250 mg	one	10 days
Uncomplicated urinary tract infections	250 mg	one	3 days

 

Step therapy can be prescribed at the discretion of the physician.

The effectiveness of this alternative regimen was noted only in infections caused by penicillin-susceptible microorganisms of Streptococcus pneumoniae , Haemophilius influenzae , of Mycoplasma pneumoniae wa hlamydia pneumoniae .

Patients with impaired renal function:

Creatinine clearance from 20 to 49 ml / min:

• an initial dose of 500 mg / day; subsequent doses of 250 mg / day.

Creatinine clearance <20 ml / min:

• initial dose of 500 mg; subsequent doses 250 mg / 48 hours

Patients with pyelonephritis and other complicated urinary tract infections:

• initial dose of 250 mg; subsequent doses of 250 mg / 48 hours.

 

Side effects

Skin reactions and general hypersensitivity reactions:sometimes: itching and redness of the skin; rarely: general hypersensitivity reactions (anaphylactic and anaphylactoid reactions) with symptoms such as urticaria, bronchoconstriction and possible severe suffocation; in rare cases: swelling of the skin and mucous membranes (for example, in the face and pharynx); very rare: sudden drop in blood pressure and shock; hypersensitivity to solar and ultraviolet radiation. In some cases: severe skin rash 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 may develop after the first dose, a few minutes or hours after the administration of Levofloxacin.

Effect on the gastrointestinal tract and metabolism: often: nausea, diarrhea; sometimes: loss of appetite, vomiting, abdominal pain, indigestion; rarely: bloody diarrhea, which in very rare cases can be a sign of intestinal inflammation and even pseudomembranous colitis; very rare: a drop in blood sugar levels (hypoglycemia), which is of particular importance for patients with diabetes mellitus; possible signs of hypoglycemia: “wolfish” appetite, nervousness, perspiration, tremors. Experience with other quinolones indicates that they are capable of exacerbating porphyria in patients already suffering from this disease. A similar effect is not excluded when using Levofloxacin.

Effect on the nervous system: sometimes: headache, dizziness and / or numbness, drowsiness, sleep disturbances; rarely: discomfort (for example, paresthesia in the hands), trembling, anxiety, fear, seizures and confusion; very rarely: visual and hearing impairments, disturbances in taste sensitivity and smell, decreased tactile sensitivity, psychotic reactions such as hallucinations and depression, as well as movement disorders, including when walking.

Effect on the cardiovascular system: rarely: increased heart rate, drop in blood pressure; very rare: (shock-like) vascular collapse.

Action on muscles, tendons and bones: rarely: tendon lesions (including tendonitis), joint and muscle pain; very rare: tendon rupture (eg, Achilles tendon). This side effect can last up to 48 hours after starting treatment and can be bilateral; muscle weakness, which is of particular importance for patients with myasthenia gravis. In some cases: muscle damage (rhabdomyolysis).

Effects on the liver and kidneys: often: increased activity of liver enzymes (for example, alanine aminotransferase and aspartate aminotransferase); sometimes: an increase in the level of bilirubin and creatinine in the blood serum (a sign of limited liver or kidney function); very rare: hepatic reactions (eg, liver inflammation); deterioration of kidney function up to acute renal failure, for example, due to allergic reactions (interstitial nephritis).

Effect on blood: Sometimes: an increase in the number of certain blood cells (eosinophilia), a decrease in the number of white blood cells (leukopenia); rare: a decrease in the number of certain white blood cells (neutropenia); a decrease in the number of platelets (thrombocytopenia), which can increase the tendency to hemorrhage or bleeding; very rare: a very strong decrease in the number of certain white blood cells (agranulocytosis), contributing to the development of severe painful symptoms (persistent or recurrent fever, sore throat, and persistent deterioration in well-being); in some cases: a decrease in the number of red blood cells due to their destruction (hemolytic anemia); a decrease in the number of blood cells of all types (pancytopenia).

Other side effects: sometimes: general weakness (asthenia); very rare: fever, allergic reactions at the level of the lungs (allergic pneumonitis) or at the level of small blood vessels (vasculitis).

Any antibiotic therapy can cause changes in the microflora (bacteria and fungi) that are normally present in humans. For this reason, an increased multiplication of bacteria and fungi that are resistant to the antibiotic used (secondary infection) may occur, which in rare cases may require additional treatment.

 

Contraindications

• individual intolerance (including a history of hypersensitivity) to levofloxacin or other quinolones;
• epilepsy;
• damage to the tendons with previous treatment with quinolones;
• children or adolescents in the growth stage (up to 18 years old) due to the likelihood of damage to the articular cartilage;
• pregnancy;
• period of breastfeeding.

 

 

 

Drug interactions

When combined with Levofloxacin taking drugs that reduce the threshold of convulsive readiness, there is a significant decrease in the threshold of convulsive readiness. The same applies to other quinolones. A decrease in the threshold is also observed when taking fenbufen, theophylline and other similar non-steroidal anti-inflammatory drugs.

With the combined use of Levofloxacin with probenecid and cimetidine, a decrease in the renal clearance of Levofloxacin is observed. Clinically, this can manifest itself only when the patient has impaired renal function (prescribe with caution).

The risk of tendon rupture increases significantly if the patient is taking glucocorticosteroids.

It is necessary to monitor the blood coagulation parameters if the patient is taking indirect anticoagulants against the background of levofloxacin.

The half-life of cyclosporin is increased with levofloxacin.

 

special instructions

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

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

In very severe pneumococcal pneumonia, levofloxacin may not provide optimal therapeutic benefits. Hospital acquired infections caused by certain pathogens (Pseudomonas aeruginosa) may require combination treatment.

During treatment with levofloxacin, a seizure attack may develop in patients with previous brain damage caused, for example, by a stroke or severe trauma. Convulsive readiness can also increase with the simultaneous use of fenbufen, similar non-steroidal anti-inflammatory drugs or theophylline a.

Despite the fact that the effect of photosensitization (hypersensitivity to light with reactions resembling sunburn) is observed very rarely when using levofloxacin, in order to avoid photosensitization, patients are not recommended to be unnecessarily exposed to strong sunlight or artificial ultraviolet irradiation (for example, exposure to the sun in highlands or a visit to the solarium).

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

Rarely observed with levofloxacin, tendonitis (primarily inflammation of the Achilles tendon) can lead to tendon rupture. Elderly patients are more prone to tendinitis. Treatment with corticosteroids (GCS) appears to increase the risk of tendon rupture. If tendonitis is suspected, treatment with levofloxacin should be discontinued immediately and the affected tendon should be treated appropriately, for example by keeping it at rest (immobilization).

Patients with glucose-6-phosphate dehydrogenase deficiency may react to quinolones by destroying red blood cells (hemolysis). In this regard, the treatment of such patients with levofloxacin should be carried out with great caution.

When prescribing levofloxacin to patients with diabetes mellitus, it is necessary to take into account the possibility of developing hypoglycemia, which will be indicated by “wolfish” appetite, nervousness, perspiration, tremors.

It is recommended to continue taking levofloxacin for at least 48–78 hours after normalization of body temperature or after reliable destruction of the pathogen. If the drug is missed, it is necessary to take the pill as soon as possible, before the time of the next dose approaches, then continue the treatment according to the scheme.

Pregnancy

Levofloxacin should not be prescribed to pregnant and lactating mothers.

Impact on the ability to drive or operate machinery

The side effects of levofloxacin, such as dizziness or numbness, drowsiness and visual disturbances, can impair reactivity and concentration. This can pose a certain risk in situations where these abilities are of particular importance (for example, when driving a car, when servicing machines and mechanisms, when performing work in an unstable position). This is especially true for cases of interaction of levofloxacin with alcohol.

 

Overdose

Symptoms of an overdose of Levofloxacin appear at the level of the central nervous system (confusion, dizziness, impaired consciousness and seizures). In addition, gastrointestinal disturbances (eg, nausea) and mucosal lesions may occur; prolongation of the QT interval (shown in studies using doses exceeding therapeutic).

Treatment should be symptom-oriented. Levofloxacin is not excreted by hemodialysis and peritoneal dialysis. There is no specific antidote.

 

Release form

Tablets 250 mg No. 10 (1×10), one blister in a cardboard box together with instructions for use.

Tablets 500 mg No. 10 (1×10), one blister in a cardboard box together with instructions for use.

Tablets 750 mg No. 5 (1×5), one blister in a cardboard box together with instructions for use.

 

Storage conditions

In a dry, dark place at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

 

Shelf life

3 years.

Do not use after the expiration date.

 

Pharmacy dispensing conditions

On prescription.