Хайлефлокс

General characteristics. Structure:

Active ingredient: 250 mg, 500 mg or 750 mg of a levofloksatsin in the form of a gemigidrat.

Excipients: starch corn, cellulose microcrystallic, K30 povidone, methylparahydroxybenzoate, пропилпарагидроксибензоат, the talc purified magnesium stearate, sodium carboxymethylstarch.

Structure of a film cover: a gipromelloza, the talc purified, a macrogoal 6000, titanium dioxide, dye a sunset yellow.

Synthetic antibacterial agent of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. Levofloxacin – synthetic фторхинолон a broad spectrum of activity. Inhibits DNK-girazu (topoisomerase II) and topoisomerase IV, breaks superspiralling and a stitching of ruptures of DNA, suppresses DNA synthesis, causes profound morphological changes in cytoplasm, a cell wall and membranes of sensitive microorganisms.

Levofloxacin is active concerning aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (leykotoksinsoderzhashchy and a coagualase - negative Methicillinum sensitive / moderately sensitive strains, including Methicillinum - sensitive strains of Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus spp. (including strains of Staphylococcus group of C and G, Streptococcus agalactiae, Streptococcus pyogenes penicillin sensitive / moderately sensitive/resistant strains of Streptococcus pneumoniae, penicillin sensitive/resistant strains of Streptococcus of the viridans group); aerobic 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 spp. (including Haemophilus ducreyi, Haemophilus parainfluenzae, ampicillin sensitive/resistant strains of Haemophilus influenzae), Helicobacter pylori, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxela catarrhalis (which are producing and not producing some β-lactamazu strains), Morganella morganii, Neisseria spp. (including Neisseria meningitidis which are producing and not producing a penicillinase Neisseria gonorroeae strains), Pasteurella spp. (including Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida), Proteus spp. (including Proteus mirabilis, Proteus vulgaris), Providencia spp. (including Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (including Pseudomonas aeruginosa), Serratia spp. (including Serratia marcescens), Salmonella spp.; anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterum spp., Veilonella spp.; other microorganisms: Bartonella spp., Chlamydia spp. (including Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis), Legionella pneumophila, Mycobacterium spp. (including Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma spp. (including Mycoplasma hominis, Mycoplasma pneumoniae), Rickettsia spp., Ureaplasma urealyticum.

Aerobic gram-positive microorganisms are steady against drug: Corynebacterium jeikeium, Staphylococcus spp. (a coagualase - negative Methicillinum - resistant strains, including Methicillinum - resistant strains of Staphylococcus aureus); aerobic gram-negative microorganisms: Alcaligenes xylosoxidans; other microorganisms: Mycobacterium avium.

Pharmacokinetics. Absorption. After oral administration levofloxacin is quickly and almost completely soaked up from a GIT. Meal influences the speed and completeness of absorption a little. Bioavailability – 99%. Cmax in plasma is reached in 1-2 h and for a levofloksatsin in doses of 250 mg, 500 and 750 mg make 2.8 mkg/ml, 5.2 mkg/ml and 8 mkg/ml respectively.

Distribution. After reception of a single or repeated dose amount of the soaked-up drug in direct ratio to the accepted dose. Css in plasma is reached in 48 h. Average Vd of a levofloksatsin varies from 74 to 112 l. Linkng with proteins of plasma of 30-40%. Well gets into bodies and fabrics: lungs, a mucous membrane of bronchial tubes, a phlegm, alveolar macrophages (concentration in tissues of lungs by 2-5 times exceeds concentration in plasma), bodies of urinogenital system, polymorphonuclear leukocytes.

Metabolism. Levofloxacin is exposed to limited metabolism in a liver (oxidation and/or a dezatsetilirovaniye).

Removal. It is brought out of an organism preferential by kidneys by glomerular filtering and canalicular secretion. T1/2 of a levofloksatsin is 6-8 h. Less than 5% of the accepted dose are removed in a look desmetil-and N-oxides-metabolites. In not changed look kidneys remove 70% of the dose accepted inside during 24 h and 87% – for 48 h 4% of the dose accepted inside is removed by intestines during 72 h.

Indications to use:

Infectious and inflammatory diseases easy and moderate severity, caused by microorganisms, sensitive to drug:

— lower respiratory tract infections (pneumonia, exacerbation of chronic bronchitis);

— acute bacterial sinusitis;

— infections of urinary tract and kidneys (including acute pyelonephritis);

— infections of skin and soft tissues (the suppurated atheromas, abscess, furuncles);

— chronic bacterial prostatitis;

— an intraabdominal infection (in a combination with the antibacterial drugs operating on anaerobic microflora);

— tuberculosis (as a part of complex therapy of drug resistant forms).

Route of administration and doses:

Inside, to food or in a break between meals, without chewing, washing down with enough water.

To adult patients with normal function of kidneys (KK> of 50 ml/min.) to apply according to the schemes presented in the table:

Infection	Dose (mg)	Frequency rate of reception in days	Duration of treatment (days)
Hospital pneumonia	750	1	7-14
Community-acquired pneumonia	500	1-2	7-14
	750	1	5 *
Acute bacterial exacerbation of chronic bronchitis	500	1	7
Acute bacterial sinusitis	500	1	10-14
	750	1	5
Uncomplicated infections of urinary tract	250	1	3
The complicated infections of urinary tract, including acute pyelonephritis	250	1	10 **
	750	1	5 ***
Uncomplicated infections of skin and hypodermic fabrics	500	1	7-10
The complicated infections of skin and hypodermic fabrics	750	1	7-14
Chronic bacterial prostatitis	500	1	28
Intraabdominal infection (in a combination with the antibacterial drugs operating on anaerobic microflora)	500	1	7-14
Tuberculosis (as a part of complex therapy of drug resistant forms)	500	1-2	Up to 3 months

* This mode is shown for treatment of the community-acquired pneumonia caused by Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Mycoplasma pneumoniae, Chlamydia pneumoniae.

** This mode is shown for treatment of infections of the urinary tract caused by Enterococcus faecalis, Enterococcus cloacae, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa and the acute pyelonephritis caused by Escherichia coli.

*** This mode is shown for treatment of infections of the urinary tract caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and the acute pyelonephritis caused by Escherichia coli including cases with the accompanying bacteremia.

Correction of a dose of a levofloksatsin at adult patients with renal failures (KK <50 ml/min.).

Dose at normal function of kidneys each 24 h	KK of 20-49 ml/min.	KK of 10-19 ml/min.	KK <10 ml/min., including at a hemodialysis or chronic out-patient peritoneal dialysis
750 mg	750 mg each 48 h	Initial dose of 750 mg, then - 500 mg each 48 h	Initial dose of 750 mg, then - 500 mg each 48 h
500 mg	Initial dose of 500 mg, then - 250 mg each 24 h	Initial dose of 500 mg, then - 250 mg each 48 h	Initial dose of 500 mg, then - 250 mg each 48 h
250 mg	Correction of a dose is not required	250 mg each 48 h. At uncomplicated infections of urinary tract correction of a dose is not required	Information on correction of a dose is absent

At an abnormal liver function correction of a dose is not required since the volume of metabolism of a levofloksatsin in a liver is limited.

Features of use:

Use at pregnancy and feeding by a breast. Drug is contraindicated at pregnancy and in the period of a lactation.

Use at abnormal liver functions. At an abnormal liver function correction of a dose is not required since the volume of metabolism of a levofloksatsin in a liver is limited.

Use at renal failures. Correction of a dose of a levofloksatsin at adult patients with renal failures (KK <50 ml/min.).

Dose at normal function of kidneys each 24 h	KK of 20-49 ml/min.	KK of 10-19 ml/min.	KK <10 ml/min., including at a hemodialysis or chronic out-patient peritoneal dialysis
750 mg	750 mg each 48 h	Initial dose of 750 mg, then - 500 mg each 48 h	Initial dose of 750 mg, then - 500 mg each 48 h
500 mg	Initial dose of 500 mg, then - 250 mg each 24 h	Initial dose of 500 mg, then - 250 mg each 48 h	Initial dose of 500 mg, then - 250 mg each 48 h
250 mg	Correction of a dose is not required	250 mg each 48 h. At uncomplicated infections of urinary tract correction of a dose is not required	Information on correction of a dose is absent

Use for children. It is contraindicated at children's and teenage age up to 18 years.

Use for elderly patients. With care patients of advanced age (high probability of existence of the accompanying depression of function of kidneys) should appoint drug.

Special instructions. After normalization of body temperature not less than 48-72 h are recommended to continue treatment.

Levofloxacin is taken not less than for 2 h to or in 2 h after reception of antacids of magnesium/aluminium, either a sukralfat, or other drugs, calciferous, by iron or zinc.

Owing to a possible photosensitization during treatment and within 5 days after the end of treatment levofloksatsiny it is necessary to avoid solar and artificial ultra-violet radiation. At phototoxicity development treatment by drug should be stopped.

At emergence of signs of a tendinitis and pseudomembranous colitis 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 the risk of hemolitic reactions is possible.

At patients with a diabetes mellitus during treatment levofloksatsiny it is necessary to watch carefully glucose level in blood.

At simultaneous use of a levofloksatsin and warfarin monitoring of a prothrombin time, MNO or other pokaztel of coagulation, and also monitoring of symptoms of bleeding is shown.

Data on use of drug of Haylefloks (750 mg) at operation of the radical or sparing sinusotomy at patients with chronic dontogenous perforative maxillary sinusitis confirms high clinical performance. Microbiological control of use of drug showed that use of drug on 750 mg of 1 times/days within 10 days suppresses a number of the aggressive bacteria capable to cause infectious complications. The received results allow to recommend drug of Haylefloks (750 mg) for the purpose of prevention of inflammatory complications of operation of the sparing sinusotomy with plastics of the oroantralny message.

Influence on ability to driving of motor transport and to control of mechanisms. Against the background of reception of a levofloksatsin ability of the patient to concentration of attention and speed of psychomotor reactions can be broken. In this regard it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity.

Side effects:

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

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

From cardiovascular system: decrease in the ABP, vascular collapse, tachycardia, lengthening of an interval of QT, ciliary arrhythmia.

From the alimentary system: nausea, vomiting, diarrhea (including with blood), digestion disturbance, a loss of appetite, an abdominal pain, pseudomembranous colitis; increase in activity of hepatic transaminases, hyperbilirubinemia, hepatitis, dysbacteriosis.

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

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

From an urinary system: giperkreatininemiya, intersticial nephrite, acute renal failure.

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

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

Others: photosensitization, adynamy, porphyria aggravation, persistent fever, development of superinfection.

Interaction with other medicines:

Levofloxacin increases cyclosporine T1/2.

The effect of a levofloksatsin is reduced by the medicines oppressing motility of intestines, сукральфат, aluminum - or magniysoderzhashchy antiacid medicines and iron preparations.

NPVS and theophylline at simultaneous use with levofloksatsiny increase risk of development of spasms in predisposed patients, and GKS increase risk of a rupture of sinews.

At a concomitant use of a levofloksatsin with hypoglycemic drugs changes of level of glucose in blood, including a hyperglycemia and a hypoglycemia are possible.

Levofloxacin strengthens effect of warfarin.

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

Contraindications:

— epilepsy;

— the damage of sinews connected with reception of hinolon in the anamnesis;

— children's and teenage age up to 18 years;

— pregnancy;

— lactation period;

— hypersensitivity to a levofoksatsin, other ftorkhinolona or other components of drug in the anamnesis.

With care should appoint drug patients of advanced age (high probability of existence of the accompanying depression of function of kidneys), at deficit glyukozo-6-fosfatdegidrogenazy.

Overdose:

Symptoms: nausea, erosive damages of mucous membranes of a GIT, lengthening of an interval of QT, confusion of consciousness, dizziness, spasms.

Treatment: a gastric lavage, if necessary – symptomatic therapy. The specific antidote does not exist, dialysis is inefficient.

Storage conditions:

Drug should be stored in the unavailable to children, dry, protected from light place, at a temperature from 8 °C to 25 °C. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

3 pieces - blisters (1) - packs cardboard.
3 pieces - blisters (10) - packs cardboard.
5 pieces - blisters (1) - packs cardboard.
5 pieces - blisters (2) - packs cardboard.
5 pieces - blisters (10) - packs cardboard.
10 pieces - blisters (1) - packs cardboard.
10 pieces - blisters (10) - packs cardboard.
100 pieces - packages polymeric (1) - banks plastic.
500 pieces - packages polymeric (1) - banks plastic.
1000 pieces - packages polymeric (1) - banks plastic.