Лефлокс

General characteristics. Structure:

Active ingredient: 250 mg of a levofloksatsin in the form of a levofloksatsin of a hemigidrat.

Excipients: microcrystallic cellulose, povidone (PVP), the water purified, carboxymethylcellulose, magnesium stearate, talc, a cover: gidroksipropilmetiltsellyuloza, isopropyl alcohol, methylene chloride, gipromelloz, iron oxide (Yellow), iron oxide (Red), talc, titanium dioxide, propylene glycol.

Antibiotic of a broad spectrum of activity from group of hinolon.

Pharmacological properties:

Pharmacodynamics. Лефлокс blocks DNK-girazu (topoisomerase II) and topoisomerase IV, breaks superspiralling and a stitching of ruptures of deoxyribonucleic acid, inhibits synthesis of deoxyribonucleic acid, causes profound metabolic changes in cytoplasm, a cell wall and membranes.

Лефлокс in vivo is active concerning the majority of strains of microorganisms as in the conditions of in vitro, and: Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, pyogenes, agalactiae, Viridans group streptococci, Enterobacter cloacae, aerogenes, agglomerans, sakazakii, Escherichia coli, Haemophilus influenzae, parainfluenzae, Klebsiella pneumoniae, oxytica, Legionella pneumoniae, Moraxella catarrhalis, Proteus miabilis, Pseudomonas aeruginosa, fluorencens, Clamydia pneumoniae, Mycoplasma pneumoniae, Acinetobacter anitatus, braumannii, calcoaceticus, Bordetella pertussis, Citrobacter diversus, freundii, Morganella morganii, Proteus vulgaris, Providencia rettgeri et stuartii, Seratia marcescens, Clostridium perfringens.

Pharmacokinetics. Лефлокс it is quickly and almost completely soaked up after oral administration. Meal influences the speed and completeness of absorption a little. Bioavailability of a lefloks after oral administration makes nearly 100%. After reception of a single dose of 500 mg of a lefloks the maximum concentration makes 5,2-6,9 mkg/ml, time of achievement of the maximum concentration - 1,3 h, an elimination half-life - 6-8 h.

Communication 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% with a stake during 72 h are allocated with urine in not changed look within 48 hours.

Indications to use:

The infections of easy or moderate severity at adults caused by the microorganisms sensitive to a levofloksatsin:
- acute sinusitis;
- chronic bronchitis in an aggravation phase;
- not hospital pneumonia;
- the complicated and uncomplicated infections of uric ways, including pyelonephritis;
- infections of skin and soft tissues;
- septicaemia/bacteremia;
- intraabdominal infections;
- prostatitis.

Route of administration and doses:

Pill is taken irrespective of meal, without chewing, washing down with a large amount of water, frequency rate of reception 1-2 times a day. Lefloks's dose depends on disease severity, type of an infection, a condition of an organism, age, weight and function of kidneys at the patient.

Duration of treatment depends on the course of a disease and should not exceed 28 days. It is recommended to continue treatment for at least 48-72 h after normalization of body temperature or the activator eradikation confirmed with results of microbiological tests. Instructions on a drug dosing at adult patients with not changed function of kidneys (clearance of creatinine — more than 50 ml/min.) are provided in the table:

Indication	Daily dose, mg	Frequency rate of receptions in days	Treatment duration, days
Acute sinusitis	500	1	10–14
Chronic bronchitis in an aggravation phase	250–500	1	7–10
Not hospital pneumonia	500–1000	1–2	7–14
Uncomplicated infections of an uric path	250	1	3
Prostatitis	500	1	28
The complicated infections of an uric path, including pyelonephritis	250	1	7–10
Infections of skin and soft tissues	500–1000	1–2	7–14
Septicaemia/bacteremia	500–1000	1–2	10–14
Intra belly infections	500	1	7–14

Instructions on a drug dosing at adult patients with an impaired renal function (clearance of creatinine — less than 50 ml/min.) are provided in the table:

Clearance of creatinine	The dosing mode (depending on weight of an infection)
50–20 ml/min.	The first dose of 250 mg, the following 125 mg / 24 h	The first dose of 500 mg, the following 250 mg / 24 h	The first dose of 500 mg, the following 250 mg / 12 h
19–10 ml/min.	The first dose of 250 mg, the following 125 mg / 48 h	The first dose of 500 mg, the following 125 mg / 24 h	The first dose of 500 mg, the following 125 mg / 12 h
<10 ml/min., (and also at a hemodialysis and HAPD *)	The first dose of 250 mg, the following 125 mg / 48 h	The first dose of 500 mg, the following 125 mg / 24 h	The first dose of 500 mg, the following 125 mg / 24 h

* After carrying out a hemodialysis or the chronic out-patient peritoneal dialysis (COPPD) of purpose of additional doses it is not required.
Dose adjustment with the broken function of a liver is not required from patients as levofloxacin is slightly metabolized in a liver.
Dose adjustment is not required from patients of advanced age at normal function of kidneys.

Features of use:

Лефлокс it is impossible to apply to treatment of children and teenagers in view of probability of damage of joint cartilages.

At treatment of patients of senile age it must be kept in mind that patients of this group often suffer from renal failures.

At the heavy pneumonia caused by pneumococci, Lefloks can not give optimum therapeutic effect. The hospital infections caused by certain activators (R. of aeruginosa), can demand the combined treatment.

During treatment by drug of Lefloks 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 readiness can increase also at simultaneous use of a fenbufen, non-steroidal anti-inflammatory drugs or theophylline, similar to it.

In spite of the fact that the photosensitization is noted at Lefloks's use very seldom, in order to avoid its patients are not recommended to be exposed without special need to power solar or artificial ultra-violet irradiation.

At suspicion of pseudomembranous colitis it is necessary to cancel immediately Lefloks and to begin the corresponding treatment. In such cases it is impossible to apply the medicines oppressing motility of intestines.

The tendinitis, seldom observable at use of drug of Lefloks (first of all an Achilles tendon inflammation) can lead to a rupture of sinews. Patients of advanced age are more inclined to a tendinitis. Treatment by corticosteroids ("kortizonovy drugs") most likely increases risk of a rupture of sinews. At suspicion on a tendinitis it is necessary to stop immediately treatment by drug of Lefloks 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 (an inherited disorder of a metabolism) 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 drug of Lefloks as dizziness or catalepsy, drowsiness and visual disturbances, can worsen reactionary ability and ability to concentration of attention.

Side effects:

From skin covers / hypersensitivity reactions: in certain cases — an itch and a dermahemia, it is rare — the general reactions of hypersensitivity (anaphylactic and anaphylactoid reactions) with such manifestations as a small tortoiseshell, a bronchospasm, heavy suffocation, a Quincke's disease of the person and mucous membrane of a throat, is very rare — sudden decrease in the ABP and shock, a photosensitization, in isolated cases — Stephens's syndrome — Johnson, a toxic epidermal necrolysis (Lyell's disease) and an exudative polymorphic erythema. Easier reactions from skin can sometimes precede system hypersensitivity reactions. The listed side effects can arise after introduction of the first dose and for several minutes or hours after reception.

From a digestive path / metabolism: often — nausea, diarrhea; in certain cases — anorexia, vomiting, an abdominal pain, dyspepsia; seldom — a bloody diarrhea who seldom or never can be display of colitis, including pseudomembranous colitis it is very rare — a hypoglycemia. Hinolona are capable to cause development of a porphyria in predisposed patients.

From a nervous system: in isolated cases — a headache, dizziness, drowsiness, frustration of a dream, it is rare — paresthesias, a tremor, concern, sensation of fear, convulsive attacks and confusion of consciousness, is very rare — a visual disturbance and hearing, taste and sense of smell, disturbances of tactile sensitivity, psychotic reactions with dangerous behavior, including suicide attempts, hallucinations, a depression, disturbances of the movement.

From cardiovascular system: seldom — tachycardia, arterial hypotension, it is very rare — a collapse.

From a musculoskeletal system: seldom — muscular weakness (especially at patients with a myasthenia), damage of sinews, including a tendinitis, a mialgiya, an arthralgia, is very rare — a rupture of a sinew, for example, Achilles (defeat can be bilateral and develop for 48 h from an initiation of treatment), in isolated cases — рабдомиолиз.

From a liver and kidneys: often — increase in activity of hepatic transaminases, in certain cases — increase in level of bilirubin and creatinine in blood serum, is very rare — hepatitis, a renal failure up to an acute renal failure (intersticial nephrite).
From system of blood: in certain cases — an eosinophilia, a leukopenia, it is rare — a neutropenia, thrombocytopenia with the increased tendency to hemorrhages, is very rare — the agranulocytosis which is followed by a long or recurrent febris, pharyngitis, etc. in isolated cases — hemolitic anemia, a pancytopenia.

Other side effects: often — pain and a dermahemia in the place of infusion, phlebitis; in certain cases — an adynamy, it is very rare — fever, an allergic pneumonitis, a vasculitis.

At use of any antibacterial agents consecutive infection which demands purpose of additional therapy can develop.

Interaction with other medicines:

There are messages on the expressed reduction of the threshold of convulsive readiness at simultaneous use of the hinolon and substances capable in turn to reduce a cerebral threshold of convulsive readiness. Equally it concerns also simultaneous use of hinolon and theophylline, a fenbufen or non-steroidal anti-inflammatory drugs, similar to it (means for treatment of rheumatic diseases).

Effect of drug of Lefloks is considerably weakened at simultaneous use with sukralfaty (means for protection of a mucous membrane of a stomach), and also at simultaneous use magnesium - or aluminum-bearing antiacid means (drugs for treatment of heartburn and gastralgias), and also iron salts (means for treatment of an anemia). Лефлокс it is necessary to accept not less, than in 2 hours prior to or in 2 hours after reception of these means. With calcium 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 probenitsid. It should be noted that this interaction has practically no clinical value. Nevertheless, at simultaneous use of medicines like probenitsid and Cimetidinum blocking a certain way of removal (canalicular secretion), treatment levofloksatsiny it is necessary to carry out with care. It concerns first of all patients with bounded function of kidneys.

Levofloxacin slightly increases a cyclosporine elimination half-life.

Reception of glucocorticosteroids increases risk of a rupture of sinews.

Contraindications:

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

Overdose:

Symptoms of overdose of drug of Lefloks are shown at the level of the central nervous system (confusion of consciousness, dizziness, disturbances of consciousness and attacks of spasms as epipripadok). Besides, gastrointestinal frustration (for example, nausea) and erosive damages of mucous membranes can be noted.

In the researches conducted by supra-therapeutic doses of Lefloks lengthening of an interval of QT was shown.

Treatment has to be oriented to the available symptoms. Лефлокс it is not removed by means of dialysis (a hemodialysis, peritoneal dialysis and continuous peritoneal dialysis). The specific antidote (counteracting substance) does not exist.

Storage conditions:

List B. To store in the place protected from moisture and light at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years.

Issue conditions:

According to the recipe

Packaging:

On 5 or 10 tablets in banks polymeric. On 5 or 10 tablets in a blister strip packaging. Bank, 1 or 2 blister strip packagings in a cardboard pack.