Levofloxacin - instructions for use, dosage, side effects, contraindications

Composition:Composition per 1 ml: active substance: levofloxacin hemihydrate (in terms of levofloxacin) - 5 mg;
auxiliary substances: sodium chloride - 9 mg, disodium edetate dihydrate - 0.1 mg, water for injection - up to 1 ml.

Description:Transparent yellowish-green liquid.

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone

ATX: & nbsp

J.01.M.A Fluoroquinolones

J.01.M.A.12 Levofloxacin

Pharmacodynamics:

Fluoroquinolone, a broad-spectrum antimicrobial bactericide. It blocks DNA-gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA gaps, inhibits DNA synthesis, causes profound morphological changes in the cytoplasm, cell wall and bacterial membranes.

Levofloxacin is active in vivo and in vitro the following microorganisms:

Aerobic Gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (at Tom number of Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (leukotoxin-containing and coagulase-negative methicillin-sensitive/moderately , sensitive strains), including Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis (methicillin-sensitive strains); Streptococcus spp. groups FROM and G, Staphylococcus agalactiae, Streptococcus pneumoniae (penicillin-sensitive/moderately sensitive/resistant strains), Streptococcus pyogenes, Streptococcus spp. groups viridans (penicillin-sensitive/resistant strains).

Aerobic Gram-negative microorganisms: Acinetobacter spp. (at Tom number of Acinetobacter baumannii), Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter spp. (at Tom number of Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (ampicillin-sensitive/resistant strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp. (at Tom number of Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella catarrhalis (producing and non-reducing beta-lactamase strains), Morganella morganii, Neisseria gonorrhoeae (producing and non-reducing penicillinase strains), Neisseria meningitidis, Pasteurella spp. (at Tom number of Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, Proteus vulgaris, Providencia spp. (at Tom number of Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (at Tom number of Pseudomonas aeruginosa), Serratia spp. (at Tom number of Serratia marcescens), Salmonella spp.

Anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterium spp., Veillonella spp.

Other microorganisms: Bartonella spp., Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella pneumophila, Mycobacterium spp. (at Tom number of Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma hominis, Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum.

Moderately sensitive microorganisms (minimal the suppressing concentration is more, 4 mg / ml):

Aerobic Gram-positive microorganisms: Corynebacterium urealyticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus - epidermis (methicillin-resistant strains), Staphylococcus haemolyticus (methicillin-resistant strains).

Aerobic Gram-negative microorganisms: Burkholderia cepacia, Campylobacter jejuni, Campilobacter coli.

Anaerobic microorganisms: Bacteroides thetaiotaomicronron, Bacteroides vulgates, Bacteroides ovatus, Prevotella spp., Porphyromonas spp.

Sustainable microorganisms (the minimum suppressive concentration is more than 8 mg / ml):

Aerobic Gram-positive microorganisms: Corynebacterium jeikeium, Staphylococcus aureus (methicillin-resistant strains), others Staphylococcus spp. (coagulase-negative methicillin-resistant strains).

Aerobic Gram-negative microorganisms: Alcaligenes xylosoxidans.

Other microorganisms: Mycobacterium avium.

Pharmacokinetics:

After intravenous infusion of 500 mg for 60 minutes, the maximum concentration (Cmah) is about 6 μg / ml. With intravenous single and repeated administration, the apparent volume of distribution after administration of the same dose is 89-112 liters.

The connection with plasma proteins is 30-40%. It penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, organs of the genitourinary system, polymorphonuclear leukocytes, alveolar macrophages.

In the liver, a small portion is oxidized and / or deacetylated.

Kidney clearance is 70% of the total clearance. The half-life (T1 / 2) is 6-8 hours.

It is excreted from the body mainly by the kidneys through glomerular filtration and tubular secretion. Less than 5 % levofloxacin is excreted as metabolites. Unchanged in the form of kidneys within 24 hours is deduced 70% and 48 hours - 87 %.

Indications:

Infectious-inflammatory diseases caused by susceptible to levofloxacin microorganisms:

- infections of the lower respiratory tract (exacerbation of chronic bronchitis, community-acquired pneumonia);

- acute maxillary sinusitis;

- uncomplicated urinary tract infections;

- complicated urinary tract infections (including acute pyelonephritis);

- infections of the skin and soft tissues (festering atheromas, abscess, boils);

- septicemia / bacteremia;

- chronic bacterial prostatitis;

- intra-abdominal infection;

- complex therapy of drug-resistant forms of tuberculosis.

Contraindications:

Hypersensitivity to levofloxacin, any other component of the drug or other drugs from the group of fluoroquinolones, epilepsy of tendon lesions with prior treatment with quinolones, pregnancy, lactation, children and adolescence (up to 18 years).

Carefully:

Elderly age (high probability of concomitant decrease in kidney function), deficiency of glucose-6-phosphate dehydrogenase.

In patients with a history of brain damage (stroke or severe trauma) (possible convulsions).

Pregnancy and lactation:

The drug is contraindicated in pregnancy.

If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

The drug is administered intravenously drip. The duration of intravenous infusion of 500 mg of levofloxacin (100 ml of infusion solution) should be at least 60 minutes.

Doses are determined by the nature and severity of the infection, as well as the suspected pathogen susceptibility.

Patients with normal renal function (creatinine clearance> 50 ml / min) the following dosage regimen is recommended:

- exacerbation of chronic bronchitis: 250-500 mg of levofloxacin once a day for 7-10 days;

- Community-acquired pneumonia: 500 mg of levofloxacin 1-2 times a day for 7-14 days;

- acute maxillary sinusitis: 500 mg of levofloxacin once a day for 10-14 days;

- Uncomplicated urinary tract infections: 250 mg of levofloxacin once a day for 3 days;

- Complicated urinary tract infections (including acute pyelonephritis): 250 mg of levofloxacin once a day for 7-10 days;

- skin and soft tissue infections: 500 mg of levofloxacin 2 times a day for 7-14 days;

- septicemia / bacteremia: 500 mg of levofloxacin 1-2 times a day for 10-14 days;

- chronic bacterial prostatitis: 500 mg of levofloxacin once a day for 28 days;

- intra-abdominal infection: 500 mg of levofloxacin once a day for 7-14 days (in combination with antibacterial drugs acting on anaerobic flora);

- complex therapy of drug-resistant forms of tuberculosis: 500 mg of levofloxacin 1-2 times a day for up to 3 months.

Patients with impaired renal function (creatinine clearance <50 mL / min) the following dosage regimen is recommended:

Clearance creatinine, ml / min	Dosages for intravenous administration
	250 mg / 24 h	500 mg / 24 h	500 mg / 12 h,
	Initial dose of 250 mg	Initial dose of 500 mg	The initial dose of 500 mg
50-20	Further 125 mg / 24 h	Then 250 mg / 24 h	Further 250 mg / 12 h
<19-10	Further 125 mg / 48 h	Further 125 mg / 24 h	Further 125 mg / 12 h
<10 (including in hemodialysis and permanent outpatient peritoneal dialysis)	Further 125 mg / 48 h	Further 125 mg / 24 h	Further 125 mg / 24 h

After hemodialysis or permanent ambulatory peritoneal dialysis (CAPD), no additional doses are required.

If the liver function is not corrected, dose adjustment is not required, since levofloxacin metabolized in the liver to an insignificant extent.

Depending on the patient's condition after a few days of treatment, it is possible to switch from intravenous drip administration to taking the same dose of the drug in a form intended for oral administration.

Side effects:

From the digestive system: nausea, vomiting, diarrhea (including blood), digestive disorders, decreased appetite, abdominal pain, pseudomembranous colitis, increased activity of "liver" transaminases, hyperbilirubinemia, hepatitis, dysbiosis.

From the cardiovascular system: decrease in arterial pressure, vascular collapse, tachycardia, increased interval QT on cardiogram, atrial fibrillation.

From the side of metabolism: hypoglycemia (increased appetite, increased sweating, trembling, nervousness), hyperglycemia.

From the side of the nervous system, headache, dizziness, weakness, drowsiness, insomnia, anxiety, paresthesia in the hands, fear, hallucinations; confusion, depression, movement disorders, convulsions.

From the sense organs: impaired vision, hearing, smell; taste and tactile sensitivity.

From the musculoskeletal system: arthralgia, muscle weakness, myalgia, tendon rupture, tendonitis, rhabdomyolysis.

From the urinary system: hypercreatininemia, interstitial nephritis, acute renal failure.

From the hematopoiesis: sometimes - eosinophilia, hemolytic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhage.

Allergic reactions: itching and hyperemia of the skin, swelling of the skin and mucous membranes, urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), bronchospasm, anaphylactic shock, allergic pneumonitis, vasculitis.

Other: asthenia, exacerbation of porphyria, photosensitivity, persistent fever, development of superinfection.

Local reactions: pain, redness at the injection site, phlebitis.

Overdose:

Symptoms: are manifested primarily from the central nervous system (confusion, dizziness, impaired consciousness and seizures as epileptic seizures).

In addition, gastrointestinal disorders (eg, nausea) and erosive lesions of the mucous membranes of the gastrointestinal tract, lengthening of the interval QT.

Treatment: symptomatic. Dialysis is ineffective. The specific antidote is not known.

Interaction:

Levofloxacin increases the half-life of cyclosporine.

Non-steroidal anti-inflammatory drugs, theophylline increase the risk development of seizures.

Admission of glucocorticosteroids increases the risk of rupture of tendons (especially in old age).

Cimetidine and drugs that block tubular secretion, slow the withdrawal of levofloxacin.

Solution for infusion is compatible with 0.9 % solution of sodium chloride, 5% dextrose solution, 2.5 % Ringer's solution with dextrose, combined solutions for parenteral nutrition (amino acids, carbohydrates, electrolytes).

Do not mix with heparin and solutions that have an alkaline reaction (for example, with sodium bicarbonate solution).

In patients with diabetes mellitus receiving oral hypoglycemic agents or insulin, against the background of taking levofloxacin hypo- and hyperglycemic conditions are possible,therefore it is recommended to control the concentration of glucose in the blood.

Levofloxacin increases the anticoagulant activity of warfarin.

Sucralfate, iron salts and magnesium- or aluminum-containing antacids reduce the effect of levofloxacin (the interval between doses should be at least 2 hours).

Alcohol can increase side effects from the central nervous system (dizziness, numbness, drowsiness).

Special instructions:

When the body temperature is normal, it is recommended to continue treatment for at least 48-72 hours.

During treatment, sunlight and artificial ultraviolet irradiation should be avoided to avoid damage to the skin (photosensitization).

When there are signs of tendinitis, pseudomembranous colitis, allergic reactions levofloxacin immediately cancel.

It should be borne in mind that the development of seizures is possible in patients with a history of brain injury (a stroke or severe trauma), if glucose-6-phosphate dehydrogenase is deficient, the risk of hemolysis of erythrocytes.

During treatment, alcohol should be avoided.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving and potentially dangerous mechanisms due to possible dizziness, drowsiness, stiffness and visual disturbances, which can lead to a slowing of the speed of psychomotor reactions and a decrease in the ability to concentrate.

Form release / dosage:

Solution for infusions 5 mg / ml.

Packaging:

100 ml in bottles of glass.

Each bottle, together with instructions for use, is placed in a pack of cardboard.

Packaging for hospitals: 56 bottles together with an equal number of instructions for use in boxes made from corrugated cardboard.

Storage conditions:

In the dark place at a temperature of 5 to 25 ° C. Freezing is unacceptable.

Keep out of the reach of children.

Shelf life:3 years.
Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-000067

Date of registration:06.12.2010

The owner of the registration certificate:OMELA, LTD. OMELA, LTD. Russia

Manufacturer: & nbsp

BELMEDPREPARATY, RUP Republic of Belarus

Information update date: & nbsp07.10.2015

Illustrated instructions

Instructions

Levofloxacin (Levofloxacin)