Levotek

General characteristics. Structure:

Active ingredient: 250,0 mg or 500,0 mg of a levofloksatsin of a gemigidrat.

Excipients: cellulose microcrystallic, starch corn, K-30 povidone, magnesium the stearate, talc purified carboxymethylstarch of sodium, silicon dioxide colloid, croscarmellose sodium.

Structure of a film cover: a gipromelloza, titanium dioxide, a macrogoal 6000, talc purified.

Antimicrobic drug of a broad spectrum of activity with pronounced bactericidal properties.

Pharmacological properties:

Pharmacodynamics. Ftorkhinolon, antibacterial (bactericidal) agent. Blocks DNK-girazu (topoisomerase II) and topoisomerase IV, breaks superspiralling and a stitching of ruptures of DNA, inhibits DNA synthesis, causes morphological changes in cytoplasm, a cell wall and membranes of bacteria.

It is effective in the relation: gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. koagulazonegativny and Methicillinum - sensitive (including moderately sensitive), including Staphylococcus aureus (Methicillinum - sensitive), Staphylococcus epidermidis (Methicillinum - sensitive), Streptococcus spp. (groups C and G), Streptococcus agalacliae, Streptococcus pneumoniae (penicillin - sensitive, moderately sensitive, resistant), Streptococcus pyogenes, Streptococcus viridans (penicillin - sensitive, moderately sensitive, resistant);

gram-negative microorganisms: Acinetobacter spp. (including Acinetobacter baumanii), Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter spp. (including Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (ampicillin - sensitive and resistant), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella catarrhalis (which are producing and not producing some beta lactamazu), Morganella morganii, Neisseria gonorrhoeae (penicillin - sensitive, moderately sensitive, resistant), Neisseria meningitidis, Pasteurella spp. (including Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (including Pseudomonas aeruginosa), Salmonella spp., Serratia spp. (including Serratia marcescens);

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

other microorganisms: Bartonella spp., Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella spp. (including Legionella pneumophila), Mycobacterium spp. (including Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma hominis, Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum/

Pharmacokinetics. Absorption. After intake it is quickly and almost completely absorbed from digestive tract, the maximum concentration is defined in plasma by 12 h. Average value of the maximum concentration after reception of 250 mg - 2.8 mkg/ml, 500 mg - 5.2 mkg/ml.

Distribution. Communication with proteins of plasma - 30-40%. Well gets into fabrics and liquids of an organism: lungs, mucous membrane of bronchial tubes, bodies of urinogenital system, bone tissue, phlegm, cerebrospinal fluid; leukocytes, macrophages. Concentration of a levofloksatsin in pulmonary fabric is higher, than in a blood plasma. The average volume of distribution of a levofloksatsin fluctuates from 89 to 112 l after one-time and multiple dose of 500 mg of drug. 24-38% of drug contact proteins of a blood plasma. Insignificant cumulation is noted only at reception of a levofloksatsin on 500 mg 2 times a day.

Metabolism. An insignificant part is exposed to hepatic metabolism (is oxidized and/or dezatsetilirutsya).

Removal. Drug is partially metabolized. An elimination half-life - 6-8 h. Also 5% - in the form of inactive metabolites within 48 hours are removed, mainly, by kidneys in not changed look (about 87%). Less than 4% - intestines within 72 hours.

Special groups of patients. Renal failure. At patients with an impaired renal function the elimination half-life of a levofloksatsin from plasma is increased that demands dose adjustment in order to avoid cumulation. Levofloxacin does not eliminirutsya from an organism by a hemodialysis or long out-patient peritoneal dialysis.

Liver failure. The abnormal liver function has no significant effect on metabolism of a levofloksatsin.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to drug:

- ENT organs (including acute antritis);
- lower respiratory, ways (exacerbation of chronic bronchitis, community-acquired pneumonia);
- urinary tract and kidneys (including acute pyelonephritis);
- bacterial prostatitis;
- infections of skin and soft tissues (the suppurated atheromas, abscess, a furunculosis);
- intraabdominal infections;
- as a part of complex therapy of drug resistant forms of tuberculosis.

Route of administration and doses:

Inside, to food or in a break between meals, without chewing, washing down with enough liquid. Duration of treatment depends on a look and weight of a course of a disease, a course of treatment - 7-14 days. After reduction of symptoms of an acute inflammation and normalization of temperature therapy levofloksatsiny continues still, at least, within 48-72 hours.

Drug dosing at patients with normal function of kidneys (clearance of creatinine> of 50 ml/min.)

Acute antritis: 500 mg of 1 times a day, within 10-14 days.

Community-acquired pneumonia: 500 mg 1-2 times a day, 7-14 days.

Exacerbation of chronic bronchitis: 250-500 mg of 1 times a day, within 7-10 days.

Uncomplicated infections of urinary tract - 250 mg of 1 times a day, a course of treatment - 3 days.

The complicated infections of urinary tract (including pyelonephritis) - 250 mg of 1 times a day (at a severe disease the dose should be increased), a course of treatment - 7-10 days.

Bacterial prostatitis - 500 mg of 1 times a day, a course of treatment - 28 days.

Infections of skin and soft tissues of-250-500 mg 2 times a day, a course lecheniya7-14 days.

Intraabdominal infection - 500 mg of 1 times a day, a course of treatment of 7-14 days (in a combination with the antibacterial drugs operating on anaerobic flora).

Complex therapy of drug resistant forms of tuberculosis - 500 mg 1-2 times a day, a course of treatment - up to 3 months.

 

Drug dosing at patients with an impaired renal function (clearance of creatinine <50 ml/min.)

 

Clearance of creatinine, ml/min.	Dosing mode
	Initial dose of 250 mg / 24 h	Initial dose of 500 mg / 24 h	Initial dose of 500 mg / 12 h
50-20	Further 125 mg / 24ч	Further 250 mg / 24 h	Further 250 mg / 12ч
19-10	Further 125 mg / 48 h	Further 125 mg / 24 h	Further 125 mg / 12 h
<10 (including at a hemodialysis and constant out-patient перитонеалыюм dialysis)	Further 125 mg / 48 h	Further 125 mg / 24 h	Further 125 mg / 24 h

After a hemodialysis or the continuous out-patient peritoneal dialysis (COPPD) introduction of additional doses is not required.

Dose adjustment is not required from patients with abnormal liver functions.

Features of use:

During treatment it is necessary to avoid solar and artificial UF of radiation in order to avoid damage of integuments (photosensitization).
It must be kept in mind that at patients with damage of a brain in the anamnesis (a stroke, a severe injury) development of spasms is possible.

At the patients receiving therapy of a hinolonama including levofloxacin, reactions of immediate hypersensitivity were in rare instances noted, up to an anaphylaxis. At emergence of signs of immediate hypersensitivity, administration of drug needs to be stopped.

At suspicion of pseudomembranous colitis it is necessary to cancel immediately levofloxacin and to begin the corresponding treatment. In such cases it is impossible to apply the medicines oppressing motility of intestines. The tendinitis which is seldom observed at drug use (first of all, the Achilles tendon inflammation) can lead to a rupture of sinews.

Patients of advanced age are more inclined to a tendinitis. Treatment of a glyukortikosteroidama increases risk of a rupture of sinews. At suspicion on a tendinitis it is necessary to stop immediately treatment levofloksatsiny and to begin the corresponding treatment of the affected sinew, for example, having provided it a condition of rest.

Patients with insufficiency glyukozo-6-fosfatdegidrogenazy can react to ftorkhinolona destruction of erythrocytes (hemolysis). In this regard treatment of such patients levofloksatsiny should be carried out carefully. Such side effects of a levofloksatsin as dizziness or catalepsy, drowsiness and visual disturbances, can worsen ability to speed of reactions and to concentration of attention that represents a certain risk in situations when these abilities have special value (for example, when driving, at service of cars and mechanisms, when working in unstable

Side effects:

From the alimentary system: nausea, vomiting, diarrhea, loss of appetite, abdominal pains, pseudomembranous colitis, increase in activity of "hepatic" transaminases, hyperbilirubinemia, hepatitis, dysbacteriosis.

From cardiovascular system: the lowering of arterial pressure, lengthening of an interval of QT, a vascular collapse, tachycardia, is extremely rare - a ciliary arrhythmia.

From a metabolism: hypoglycemia (increase in appetite, sweating, nervousness, shiver).

From a nervous system: headache, dizziness, weakness, drowsiness, sleeplessness, paresthesias, concern, fear, hallucinations, confusion of consciousness, depression, motive frustration, spasms.

From sense bodys: vision disorders, hearing, sense of smell, flavoring and tactile sensitivity.

From a musculoskeletal system: arthralgia, mialgiya, myasthenia, rupture of sinews, рабдомиолиз, tendinitis.

From an urinary system: giperkreatininemiya, intersticial nephrite.

From bodies of a hemopoiesis: eosinophilia, hemolitic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhages.

Allergic reactions: itch, cutaneous dropsy and mucous membranes, small tortoiseshell, malignant exudative erythema (Stephens-Johnson's syndrome), toxic epidermal necrolysis (Lyell's disease), bronchospasm, acute anaphylaxis, allergic pneumonitis, vasculitis.

Others - a porphyria aggravation, a photosensitization, persistent fever, development of superinfection.

Interaction with other medicines:

Drug increases a cyclosporine elimination half-life.

At simultaneous use of antagonists of vitamin K control of coagulant system of blood is necessary.

Cimetidinum and medicines blocking canalicular secretion slow down removal.

The effect is reduced by the medicines oppressing motility of intestines, сукральфат, magnesium or aluminum-bearing antiacid means, salts ~ iron and zinc (the break between reception not less than 2 h is necessary).

Hypoglycemic drugs: strict control of glucose level in blood as there is a probability hyper - and a hypoglycemia at their simultaneous use with levofloksatsiny is necessary.

Non-steroidal anti-inflammatory drugs and theophylline: at use with levofloksatsiny increase convulsive readiness.

Glucocorticosteroids: increase risk of a rupture of sinews.

Contraindications:

Hypersensitivity to a levofloksatsin, other ftorkhinolona or other components of drug, epilepsy, damage of sinews at earlier carried out treatment of a hinolonama, pregnancy, the lactation period, children's and teenage age (up to 18 years).

With care: to elderly people, at deficit glyukozo-6-fosfatdegidrogenazy.

Overdose:

Symptoms: gastrointestinal frustration (nausea), erosive damages of a mucous membrane of digestive tract, change of an interval of QT, confusion of consciousness, dizziness, spasms.

Treatment: symptomatic therapy, dialysis it is not effective, the specific antidote is not known.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated 250 mg and 500 mg. 10 tablets, film coated in planimetric PVC / aluminum packaging (blister). 1 or 10 planimetric packagings (blisters) in a pack cardboard, together with the instruction on a medical use.