LEVOPIR [Levofloxacin] 500 mg Film-coated tablets
LEVOPIR
instructions for medical use of the medicinal product
Tradename
Levopir, Levopir
International non-proprietary name
Levofloxacin, Levofloxacin
Composition
Levopir 250 mg
Each film-coated tablet contains:
active substance: levofloxacin USP 250 mg
Excipients: corn starch, microcrystalline cellulose, sodium starch glycolate, 10% starch paste, magnesium stearate; film shell: titanium oxide, talc, hydroxypropyl methylcellulose, polyethylene glycol, polyvinyl glycol.
Levopir 500 mg
Each film-coated tablet contains:
active substance: levofloxacin USP 500 mg
excipients: corn starch, microcrystalline cellulose, sodium starch glycolate, 10% starch paste, magnesium stearate, titanium oxide, talc, hydroxypropyl methylcellulose, polyethylene glycol, polyvinyl glycol.
Dosage form
Tablets.
Pharmacotherapeutic group
The antimicrobial agent is a fluoroquinolone.
Pharmacological properties
Levopir is a synthetic broad-spectrum antibacterial drug from the group of fluoroquinolones containing levofloxacin as an active substance.
Pharmacodynamics
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.
Sensitive microorganisms
Aerobic gram-positive microorganisms: Bacillus anthracis, Staphylococcus aureus methicillin-sensitive, Staphylococcus saprophyticus, Streptococci groups C and G, Streptococcus agalactiae, Streptococcus pneumonia, Streptococcus pyogenes .
Aerobic gram-negative microorganisms: Eikenella corrodens, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella oxytoca, Moraxela catarrhalis, Pasteurella multocida, Proteus vulgaris, Providencia rettgeri .
Anaerobic microorganisms: Peptostreptococcus .
Other microorganisms: Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella pneumophila, Mycoplasma hominis, Mycoplasma pneumoniae, Ureaplasma urealyticum .
Microorganisms that can become resistant
Aerobic gram-positive microorganisms: Enterococcus faecalis, Staphylococcus aureus methicillin-resistant, coagulase-negative Staphylococcus spp .
Aerobic gram-negative microorganisms: Acinetobacter baumanii, Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Klebsiella pneumonia, Morganella morganii, Proteus mirabilis, Providencia stuartii, Pseudomonas aeruginosa, Serratia marcescens .
Anaerobic microorganisms: Bacteroides fragilis .
Levofloxacin-resistant microorganisms
Aerobic gram-positive microorganisms: Enterococcus faecium .
Due to the peculiarities of the mechanism of action of levofloxacin, there is usually no cross-resistance between levofloxacin and other antimicrobial agents.
Pharmacokinetics
Levofloxacin is rapidly and almost completely absorbed after oral administration. Food intake has little effect on the rate 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, C max is 5.2-6.9 μg / ml, the time to reach C max is 1.3 hours, T 1/2 is 6-8 hours.
Plasma protein binding - 30-40%. It penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, organs of the genitourinary system, bone tissue, cerebrospinal fluid, prostate gland, polymorphonuclear leukocytes, alveolar macrophages.
In the liver, a small part is oxidized and/or deacetylated. It is excreted from the body mainly 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. As renal function declines, renal excretion and renal clearance decrease and the half-life increases.
Indications for use
- acute sinusitis;
- exacerbation of chronic bronchitis;
- community-acquired pneumonia;
- pyelonephritis and complicated urinary tract infections;
– 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, other quinolones;
- epilepsy;
- severe renal failure;
- tendon lesions associated with the use of fluoroquinolones in history;
- children and adolescents up to 18 years;
- pregnancy;
- period of breastfeeding.
Dosage and administration
inside. Swallow the tablets whole with water during meals or at any time between meals 1 or 2 times / day.
Doses are determined by the nature and severity of the infection, as well as the sensitivity of the suspected pathogen. The following dosing regimen is recommended:
Acute sinusitis: 250 mg 2 times a day or 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 once a day, 3 days;
Prostatitis: 500 mg once a 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 per day or 500 mg 1-2 times a day, 7-14 days;
Septicemia / bacteremia: 250 mg or 500 mg 1-2 times a day, 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 the anaerobic flora).
For patients with impaired renal function and elderly patients, the dosage of Levopyr tablets should be adjusted depending on the degree of impairment.
As with other antibiotics, treatment with Levopyr is recommended to continue for at least 48-78 hours after normalization of body temperature or after laboratory-confirmed recovery.
Special instructions and precautions
The use of Levopyr should be avoided in patients with a history of serious adverse reactions associated with taking quinolone or fluoroquinolone-containing drugs. Treatment of such patients with Levopyr should only be started if there are no alternative treatment options and after a careful assessment of the benefit/risk ratio.
At the first signs or symptoms of any serious adverse reactions (eg, swelling, pain in the tendon area, joint and muscle pain, burning sensation, tingling sensation, weakness or pain in the limbs, confusion, convulsions, severe headache, or hallucinations), immediately stop treatment and consult a doctor.
Levopir should not 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.
With severe inflammation of the lungs caused by pneumococci, Levopir may not give the optimal therapeutic effect. Hospital infections caused by certain pathogens (P. aeruginosa) may require combined treatment.
During treatment with Levopyr, seizures may develop in patients with previous brain damage, such as a stroke or severe trauma.
It is not recommended during treatment to be subjected to unnecessarily strong solar or artificial ultraviolet radiation in order to avoid photosensitivity.
If pseudomembranous colitis is suspected, Levopir should be immediately discontinued and appropriate treatment initiated. In such cases, drugs that inhibit intestinal motility should not be used.
If tendinitis is suspected, treatment with Levopyr 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, the treatment of such patients with Levopyr should be carried out with great caution.
Influence on the ability to drive vehicles and mechanisms
During the period of treatment, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.
Use during pregnancy and during breastfeeding
Use during pregnancy and during breastfeeding is contraindicated.
Interaction with other drugs
The absorption of levofloxacin is significantly reduced with the concomitant use of iron salts, magnesium or aluminum-containing antacids, didanosine. Taking fluoroquinolones together with multivitamin preparations containing zinc reduces their absorption when taken orally. Preparations containing di- and trivalent cations, such as iron salts, zinc salts, magnesium- or aluminum-containing antacids, didanosine (only products with didanosine containing aluminum or magnesium as buffer substances) are recommended to be taken at least 2 hours before or after 2 hours after taking levofloxacin.
Calcium salts have a minimal effect on the absorption of levofloxacin when taken orally.
The action of levofloxacin is significantly weakened with the simultaneous use of sucralfate (means to protect the gastric mucosa). It is recommended to take sucralfate 2 hours after taking levofloxacin.
With the simultaneous use of quinolones and theophylline, NSAIDs and other drugs that reduce the threshold for convulsive readiness of the brain, a pronounced decrease in the threshold for convulsive readiness of the brain is possible.
In patients treated with levofloxacin in combination with indirect anticoagulants (for example, warfarin), an increase in prothrombin time and / or development of bleeding, including severe, was observed. Therefore, with the simultaneous use of indirect anticoagulants and levofloxacin, regular monitoring of blood coagulation parameters is necessary.
With the simultaneous use of levofloxacin with drugs that violate renal tubular secretion, such as probenecid and cimetidine, caution should be exercised, especially in patients with renal insufficiency.
Simultaneous reception with glucocorticosteroids increases the risk of tendon rupture.
Levofloxacin, like other fluoroquinolones, should be used with caution in patients receiving drugs that prolong the QT interval (eg, class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, antipsychotics).
Side effect
The frequency of this or that side effect is determined as follows: often (> 10%) ; sometimes (1-10%) ; rarely (0.1-1%) ; very rarely (0.01-0.1%) ; individual cases (less than 0.01%).
Allergic reactions: sometimes - itching and redness of the skin; rarely - general hypersensitivity reactions (anaphylactic and anaphylactoid reactions) with symptoms such as urticaria, bronchial constriction and, possibly, severe suffocation; very rarely - swelling of the skin and mucous membranes (for example, in the face and pharynx), a sudden drop in blood pressure and shock, increased sensitivity to sunlight and ultraviolet radiation, allergic pneumonitis, vasculitis; in some cases, severe rashes on the skin with the formation of blisters, 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 the administration of the drug.
From the digestive system: often - nausea, diarrhea, increased activity of liver enzymes (for example, ALT and AST); sometimes - loss of appetite, vomiting, abdominal pain, indigestion; rarely - diarrhea mixed with blood, which in very rare cases can be a sign of intestinal inflammation and even pseudomembranous colitis.
From the side of metabolism: very rarely - a decrease in the concentration of glucose in the blood, which is of particular importance for patients with diabetes mellitus (possible signs of hypoglycemia: increased appetite, nervousness, perspiration, trembling). Can cause exacerbation of porphyria in patients suffering from this disease.
From the nervous system: sometimes - headache, dizziness and / or numbness, 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 side of the cardiovascular system: rarely - increased heart rate, decreased blood pressure; very rarely - vascular (shock-like) collapse; in some cases - prolongation of the QT interval.
From the musculoskeletal system: rarely - tendon lesions (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, muscle weakness, which is of particular importance for patients with bulbar syndrome; in some cases - muscle damage (rhabdomyolysis).
From the urinary system: very rarely - deterioration of kidney function up to acute renal failure, interstitial nephritis.
On the part of 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 fever, deterioration of health); in some cases - hemolytic anemia; pancytopenia.
Others: sometimes - general weakness; rarely - an increase in the level of bilirubin and creatinine in the blood serum; very rarely - fever.
Overdose
Symptoms:
nausea, vomiting, dizziness, confusion, convulsions.
Treatment: gastric lavage and administration of antacids should be performed to protect the gastric mucosa. Levopir is eliminated by dialysis (hemodialysis, peritoneal dialysis and continuous ambulatory peritoneal dialysis). The specific antidote is not known.