Levotek

General characteristics. Structure:

Active ingredient: 5 mg of a levofloksatsin in an equivalent of a levofloksatsin of a gemigidrat of 5,12 mg in 1 ml of solution (500 mg of a levofloksatsin in 100 ml).

Excipients: glucose anhydrous, sodium hydroxide, hloristovodoyorodyony acid, water for injections.

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

Pharmacological properties:

Pharmacodynamics. Antimicrobic broad-spectrum agent, фторхинолон. Works bakteritsidno. Blocks DNK-girazu (topoisomerase II) and topoisomerase IV, breaks superspiralling and a stitching of ruptures of DNA, inhibits DNA synthesis, causes profound morphological changes in cytoplasm, a cell wall and membranes.

Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes and Streptococcus agalactiae, Viridans group streptococci, Enterobacter cloacae, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter sakazakii, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Klebsiella oxytoca, Legionella pneumoniae, Moraxella catarrhalis, Proteus mirabilis, Pseudomonas aeruginosa, Pseudomonas fluorescens, Chlamydia pneumoniae, Mycoplasma pneumoniae, Acinetobacter anitratus, Acinetobacter baumannii, Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter diversus, Citrobacter freundii, Morganella morganii, Proteus vulgaris, Providencia rettgeri, Providcncia stuartii, Serratia marcescens, Clostridium perfringens is active concerning Enterococcus faecalis.

Pharmacokinetics. At intake it is absorbed from a GIT quickly and almost completely. Meal influences the speed and completeness of absorption a little. Bioavailability makes 99%. Cmax is reached in 1-2 h and at reception of 250 mg and 500 mg makes 2.8 and 5.2 mkg/ml respectively. Linkng with proteins of plasma - 30-40%. Well gets into bodies and fabrics: lungs, mucous membrane of bronchial tubes, phlegm, bodies of urinogenital system, polymorphonuclear leukocytes, alveolar macrophages. In a liver a small part is oxidized and/or dezatsetilirutsya. The renal clearance makes 70% of the general clearance.

T1/2 is 6-8 h. It is brought out of an organism preferential by kidneys by glomerular filtering and canalicular secretion. Less than 5% of a levofloksatsin are excreted in the form of metabolites. In not changed view with urine during 24 h 70% and for 48 h - 87% are removed; in Calais for 72 h 4% of the dose accepted inside are found. Later in/in infusion of 500 mg within 60 min. Cmax - 6.2 mkg/ml. At in single and repeated introduction the seeming Vd after introduction of the same dose makes 89-112 l, Cmax - 6.2 mkg/ml, T1/2 - 6.4 h.

Indications to use:

Infections of lower parts of respiratory tracts (chronic bronchitis, pneumonia), ENT organs (sinusitis, average otitis), urinary tract and kidneys (including acute pyelonephritis), generative organs (including urogenital clamidiosis), skin and soft tissues (the suppurated atheromas, abscess, furuncles).

Route of administration and doses:

Apply inside or in / century.

At sinusitis - inside, on 500 mg of 1 times/days; at an exacerbation of chronic bronchitis - on 250-500 mg of 1 times/days. At pneumonia - inside, on 250-500 mg of 1-2 times/days (500-1000 mg/days); in/in - on 500 mg of 1-2 times/days. At infections of urinary tract - inside, 250 mg of 1 times/days or in/in in the same dose. At infections of skin and soft tissues - on 250-500 mg in 1-2 times/days or in/in, on 500 mg of 2 times/days. Later in/in introductions in several days transition to intake in the same dose is possible.

At diseases of kidneys the dose is reduced according to extent of dysfunction: at ml/min. KK=20-50 - on 125-250 mg of 1-2 times/days, at ml/min. KK=10-19 - 125 mg of 1 times in 12-48 h, at KK <10 ml/min. - 125 mg in 24 or 48 h. Treatment duration - 7-10 (to 14) days.

Features of use:

With care apply levofloxacin to patients of advanced age (high probability of existence of the accompanying depression of function of kidneys).

After normalization of temperature it is recommended to continue treatment not less than 48-78 h. Duration in/in injections of 500 mg (100 ml of infuzioiny solution) has to make not less than 60 min. During treatment it is necessary to avoid solar and artificial UF of radiation in order to avoid damage of integuments (photosensitization). At emergence of signs of a tendinitis levofloxacin is immediately cancelled. 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 insufficiency glyukozo-6-fosfatdegidrogenazy - risk of development of hemolysis.

Influence on ability to driving of motor transport and to control of mechanisms. During treatment it is necessary to abstain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

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

From cardiovascular system: decrease in the ABP, vascular collapse, tachycardia.

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

From TsNS and peripheral nervous system: headache, dizziness, weakness, drowsiness, sleeplessness, paresthesias, uneasiness, 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, rupture of sinews, muscular weakness, tendinitis.

From an urinary system: giperkreatininemiya, intersticial nephrite.

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

Dermatological reactions: photosensitization, itch, cutaneous dropsy and mucous membranes, malignant exudative erythema (Stephens-Johnson's syndrome), toxic epidermal necrolysis (Lyell's disease).

Allergic reactions: small tortoiseshell, bronchospasm, suffocation, acute anaphylaxis, allergic pneumonitis, vasculitis.

Others: porphyria aggravation, рабдомиолиз, persistent fever, development of superinfection.

Interaction with other medicines:

Levofloxacin increases cyclosporine T1/2.

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

At simultaneous use of NPVS, theophylline increase convulsive readiness, GKS - increase risk of a rupture of sinews.

Cimetidinum and medicines blocking canalicular secretion slow down removal of a levofloksatsin.

Solution of a levofloksatsin for in/in introductions is compatible from 0.9% solution of sodium of chloride, 5% solution of a dextrose, 2.5% Ringer's solution to a dextrose, the combined solutions for parenteral food (amino acids, carbohydrates, electrolytes).

Solution of a levofloksatsin for in/in introductions cannot be mixed with the heparin and solutions having alkali reaction.

Contraindications:

Hypersensitivity, epilepsy, damage of sinews at earlier carried out treatment of a hinolonama, pregnancy, a lactation, children's and teenage age up to 18 years.

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:

List B. In the dry, protected from light place at a temperature not over 25 ºС. Not to freeze. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

100 ml - bottles polyethylene (1) - packages polypropylene (1) - packs cardboard.