Элефлокс

General characteristics. Structure:

Tablets, film coated 1 table.
levofloksatsina гемигидрат 256,38 mg
(it is equivalent to a levofloksatsin — 250 mg) 
in the blister of 5 pieces; in a pack cardboard 1 or 2 blisters.

Tablets, film coated 1 table.
levofloksatsina гемигидрат 512,76 mg
(it is equivalent to a levofloksatsin — 500 mg)  
in blisters on 5 pieces; in a pack cardboard 1 or 2 blisters.

Description. Tablets of Elefloks of 250 mg: flesh-colored color, biconvex, an oval form, film coated, with engraved "250" on one party.
Tablets of Elefloks of 500 mg: flesh-colored color, biconvex, an oval form, coated, with engraved "500" on one party.

Pharmacological properties:

Pharmacokinetics. Levofloxacin is quickly and almost completely soaked up after oral administration. Meal influences the speed and completeness of absorption a little. Bioavailability of a levofloksatsin after oral administration in a dose of 500 mg makes nearly 100%. After reception of a single dose of 500 mg of a levofloksatsin of Cmax makes 5,2–6,9 mkg/ml, Tmax is 1,3 h, T1/2 is 6–8 h.
Linkng with proteins of plasma — 30–40%. Well gets into bodies and fabrics: lungs, mucous membrane of bronchial tubes, phlegm, bodies of urinogenital system, bone tissue, cerebrospinal fluid, prostate, polymorphonuclear leukocytes, alveolar macrophages.
In a liver a small part is oxidized and/or dezatsetilirutsya. It is brought out of an organism preferential by kidneys by glomerular filtering and canalicular secretion. After oral administration about 87% of the accepted dose less than 4% — intestines during 72 h are allocated with kidneys in not changed look during 48 h.

Pharmacodynamics. Элефлокс — the synthetic antibacterial drug of a broad spectrum of activity from group of ftorkhinolon containing levofloxacin in quality of active agent — left-handed isomer of an ofloksatsin. Levofloxacin blocks DNK-girazu, breaks superspiralling and a stitching of ruptures of DNA, inhibits DNA synthesis, causes profound morphological changes in cytoplasm, a cell wall and membranes of bacteria. Levofloxacin is active concerning the majority of strains of microorganisms as in the conditions of in vitro, and in vivo.
Sensitive microorganisms (MPK of ≤2 mg/l):
Aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp., koagulazonegativny metitsillinochuvstviteljnye/-moderately sensitive (including Staphylococcus aureus metitsillinochuvstvitelny, Staphylococcus epidermidis metitsillinochuvstvitelny), Streptococcus spp. (groups C and G), Streptococcus agalactiae, Streptococcus pneumoniae penitsillinochuvstvitelnye/-moderately sensitive / - resistant, Streptococcus pyogenes, Streptococcus spp. the viridans groups are penitsillino-chuvstvitelnye/-resistant.
Aerobic gram-negative mikroorganizmy:acinetobacter spp. (including Acinetobacter baumanii), Citrobacter freundii, Eikenella corrodens, Enterobacter spp. (in t.ch.enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae ampitsillinochuvstvitelnye/-resistant, Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp. (including Klebsiella pneumoniae, Klebsiella oxytoca), Moraxella catarrhalis (which are producing and not producing some beta lactamazu strains), Morganella morganii, Neisseria gonorrhoeae (including producing a penicillinase), Neisseria meningitidis, Pasteurella spp. (including Pasteurella multocida, Pasteurella dagmatis, Pasteurella canis), Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia stuartii, Providencia rettgeri), Pseudomonas spp. (including Pseudomonas aeruginosa), Salmonella spp., Serratia spp. (including Serratia marcescens).
Anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus, 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, Rickettsiae spp., Ureaplasma urealyticum.
Moderately sensitive (MPK of ≥4 mg/l):
Aerobic gram-positive microorganisms: Corynebacterium urealyticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis metitsillinorezistentny, Staphylococcus haemolyticus metitsillinorezistentny.
Aerobic gram-negative microorganisms: Burkholderia cepacia, Campilobacter jejuni, Campilobacter coli.
Anaerobic microorganisms: Bacteroides thetaiotaomicron, Bacteroides vulgatus, Bacteroides ovatus, Prevotella spp., Porphyromonas spp.
Steady (MPK of ≥8 mg/l):
Aerobic gram-positive microorganisms: Corynebacterium jeikeium, Staphylococcus aureus metitsillinorezistentny, other Staphylococcus spp. koagulazonegativny metitsillinorezistentny.
Aerobic gram-negative microorganisms: Alcaligenes xylosoxidans.
Other microorganisms: Mycobacterium avium.

Indications to use:

The infectious and inflammatory diseases caused by sensitive microorganisms:
● ENT organs (including acute antritis);
● lower respiratory tracts (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, before food or between meals, without chewing 1–2 times a day and washing down with enough liquid. Doses are defined by character and weight of an infection, and also sensitivity of the estimated activator.
More than 50 ml/min. are recommended to patients with creatinine Cl the following mode of dosing:
- acute antritis: on 500 mg once a day — 10–14 days;
- exacerbation of chronic bronchitis: on 250 mg or on 500 mg once a day — 7–10 days;
- community-acquired pneumonia: on 500 mg 1–2 times a day — 7–14 days;
- uncomplicated infections of urinary tract: on 250 mg once a day — 3 days;
- the complicated infections of urinary tract (including pyelonephritis): on 250 mg once a day — 7–10 days (at a severe disease the dose should be increased);
- bacterial prostatitis: on 500 mg once a day — 28 days;
- infections of skin and soft tissues: on 250–500 mg — 1–2 times a day — 7–14 days;
- intraabdominal infection: on 500 mg once a day — 7–14 days (in a combination with the antibacterial drugs operating on anaerobic flora);
- complex therapy of drug resistant forms of tuberculosis: on 500 mg 1–2 times a day, a course of treatment — up to 3 months.
The dosing mode at patients with an impaired renal function:
The dosing mode at patients with an impaired renal function
 Clearance of creatinine of 250 mg / 24 h 500 mg / 24 h 500 mg / 12 h
 first dose of 250 mg first dose of 500 mg first dose of 500 mg
50–20 ml/min. then 125 mg / 24 h then 250 mg / 24 h then 250 mg / 12 h
19–10 ml/min. then 125 mg / 48 h then 125 mg / 24 h then 125 mg / 12 h
 <10 ml/min., including a hemodialysis and PAPD * then 125 mg / 48 h then 125 mg / 24 h then 125 mg / 24 h
* PAPD — continuous out-patient peritoneal dialysis.
After a hemodialysis or PAPD introduction of additional doses is not required.
At an abnormal liver function special selection of doses as levofloxacin is only slightly metabolized in a liver is not required.
Patients of advanced age do not need change of the mode of dosing, except for cases of low clearance of creatinine.
As well as at use of other antibiotics, treatment levofloksatsiny it is necessary to continue not less than 48-72 p after normalization of body temperature or after reliable destruction of activators.
If administration of drug is missed, it is necessary to take as soon as possible a pill, time of the next reception did not come yet. Further it is necessary to accept drug according to the scheme.

Features of use:

At treatment of persons of senile age it must be kept in mind that patients of this group often suffer from renal failures (see the section "Route of Administration and Doses").
During treatment by drug of Elefloks development of an attack of spasms in patients with the previous damage of a brain caused, for example, by a stroke or a severe injury is possible. Convulsive activity can increase also at simultaneous use of a fenbufen and other NPVS or theophylline (see. "Interaction").
In spite of the fact that the photosensitization is noted at use of a levofloksatsin very seldom, in order to avoid it, patients are not recommended to be exposed to solar and artificial UF-radiation.
At suspicion of pseudomembranous colitis it is necessary to cancel immediately Elefloks and to begin the corresponding treatment. In such cases it is impossible to apply the HP oppressing motility of intestines.
At suspicion on a tendinitis it is necessary to stop immediately treatment by drug of Elefloks 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 with care.
In the course of any antibioticotherapia normal microflora (bacteria and mushrooms), sensitive to the appointed drugs, is suppressed. For this reason consecutive infection or superinfection which can demand additional treatment can develop.
During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Frequency of emergence of this or that side effect is defined as follows: often — at 1–10 patients from 100; sometimes — less than at 1 patient from 100; seldom — less than at 1 patient from 1000; very seldom — less than at 1 patient from 10000; in some cases — less than at 1 patient from more than 10000.
From the alimentary system: often — nausea, diarrhea, increase in activity of enzymes of a liver (for example ALT and nuclear heating plant); sometimes — a loss of appetite, vomiting, abdominal pains, digestion disturbance; seldom — diarrhea (including with blood) which seldom or never can be a sign of an inflammation of intestines and even pseudomembranous colitis (see the section "Special Instructions"), increase in level of bilirubin in blood serum, dysbacteriosis; very seldom — hepatitis.
From a nervous system: sometimes — a headache, dizziness, drowsiness, sleep disorders; seldom — a depression, concern, psychotic reactions (for example with hallucinations), unpleasant feelings (for example paresthesias in hands), a shiver, the excited state, spasms and confusion of consciousness; very seldom — a vision disorder and hearing, disturbances of flavoring sensitivity and sense of smell, decrease in tactile sensitivity.
From cardiovascular system: seldom — tachycardia, decrease in the ABP; very seldom — a vascular collapse; in some cases — lengthening of an interval of QT, a ciliary arrhythmia.
From a metabolism: very seldom — the decrease in concentration of glucose in blood (hypoglycemia) having special value for patients with a diabetes mellitus with symptoms: the increased appetite, nervousness, sweating, a shiver.
From a musculoskeletal system: seldom — damages of sinews (including a tendinitis), an arthralgia, a mialgiya; very seldom — a rupture of sinews (for example an Achilles tendon), muscular weakness; in some cases — damage of muscles (рабдомиолиз).
From an urinary system: very seldom — a giperkreatininemiya, intersticial nephrite, an acute renal failure.
From bodies of a hemopoiesis: sometimes — an eosinophilia, a leukopenia; seldom — a neutropenia; thrombocytopenia, hemorrhages; very seldom — an agranulocytosis; in some cases — hemolitic anemia, a pancytopenia.
Allergic reactions: sometimes — an itch and erubescence; seldom — the general reactions of hypersensitivity (anaphylactic and anaphylactoid reactions) with such symptoms as a small tortoiseshell, a bronchospasm and a laryngospasm, heavy suffocation; seldom or never — cutaneous dropsies and mucous membranes (for example in a face and a throat), an acute anaphylaxis, an allergic pneumonitis, a vasculitis; in some cases — a heavy enanthesis with formation of bubbles, for example Stephens-Johnson's syndrome, a toxic epidermal necrolysis (Lyell's disease) and an exudative mnogoformny erythema.
Others: sometimes — the general weakness (adynamy); very seldom — a porphyria aggravation, fever, a photosensitization, development of superinfection.

Interaction with other medicines:

Hinolona in combination with drugs which reduce a threshold of convulsive activity (for example with theophylline, fenbufeny and other NPVS) can cause the expressed reduction of the threshold of convulsive activity.
The effect of drug of Elefloks is considerably weakened at simultaneous use with sukralfaty. The same occurs also at simultaneous use magnesium - or aluminum-bearing antiacid means, and also iron salts. Элефлокс it is necessary to take not less than for 2 h to or in 2 h after reception of these means. From calcium by a carbonate of interaction it is not revealed.
At simultaneous use of antagonists of vitamin K control of coagulant system of blood is necessary.
Removal (renal clearance) of a levofloksatsin is slightly slowed down under the influence of Cimetidinum and a probenetsid.
At a combination to hypoglycemic drugs strict control of concentration of glucose in blood since there is a probability hyper - and a hypoglycemia is necessary.
Levofloxacin slightly increases cyclosporine T1/2.
Reception of GKS increases risk of a rupture of sinews.

Contraindications:

Hypersensitivity to a levofloksatsin or other hinolona;
● epilepsy;
● damage of sinews at earlier carried out treatment of a hinolonama;
● children's and teenage age (up to 18 years);
● pregnancy;
● lactation period.

With care: to elderly people, at deficit glyukozo-6-fosfatdegidrogenazy, at an impaired renal function.

Overdose:

Symptoms: are shown preferential from TsNS (confusion of consciousness, dizziness and attacks of spasms as epileptic seizures). Besides, gastrointestinal frustration (for example nausea) and erosive damages of a mucous membrane of a GIT, lengthening of an interval of QT can be noted.
Treatment: symptomatic. Levofloxacin is not removed by means of dialysis (a hemodialysis, peritoneal dialysis and continuous peritoneal dialysis). The specific antidote does not exist.

Storage conditions:

Tab. of pct of the lake of 250 mg, бл.; tab. of pct of the lake of 500 mg, бл. — in the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity. Tab. of pct of the lake of 250 mg, бл.; tab. of pct of the lake of 500 mg, бл. — 3 years.

Issue conditions:

According to the recipe