Ekotsifol

General characteristics. Structure:

Active agents: ciprofloxacin (in the form of a monohydrate hydrochloride) 500 mg

Excipients: lactulose - 600 mg, povidone low-molecular - 28 mg, croscarmellose sodium - 65 mg, cellulose microcrystallic - 60 mg, magnesium stearate - 10 mg, starch corn - to 1400 mg.

Structure of a film cover: (a gipromelloza - 19.04 mg, a macrogoal-4000 - 8.32 mg, talc - 2.2 mg, titanium dioxide - 10.44 mg) - to 1440 mg.

Pharmacological properties:

Pharmacodynamics. The antimicrobic broad-spectrum agent derivative of a hinolon, suppresses bacterial DNK-girazu (the topoisomerases II and IV responsible for process of superspiralling of chromosomal DNA around nuclear RNA that is necessary for reading of genetic information), breaks DNA synthesis, growth and division of bacteria; causes the expressed morphological changes (including a cell wall and membranes) and bystry death of a bacterial cell.
Affects bakteritsidno gram-negative organisms during a dormant period and divisions (since influences not only on DNK-girazu, but also causes a lysis of a cell wall), on gram-positive microorganisms - only during division.
The hypotoxicity for cells of a macroorganism is explained by absence in them DNK-girazy. Against the background of reception of ciprofloxacin there is no parallel development of resistance to other aktibiotika which are not belonging to group of DNK-girazy inhibitors that does it highly effective in relation to bacteria which are steady, for example to aminoglycosides, penicillin, cephalosporins, tetracyclines.
Gram-negative aerobic bacteria are sensitive to ciprofloxacin: enterobakteriya (Escherichia coli, Salmonella spp., Shigella spp., Citrobacter spp., Klebsiella spp., Enterobacter spp., Proteus mirabilis, Proteus vulgaris, Serratia marcescens, Hafnia alvei, Edwardsiella tarda, Providencia spp., Morganella morganii, Vibrio spp., Yersinia spp.), other gram-negative bacteria (Haemophilus spp., Pseudomonas aeruginosa, Moraxella catarrhalis, Aeromonas spp., Pasteurella multocida, Plesiomonas shigelloides, Campylobacter jejuni, Neisseria spp.); some intracellular activators: Legionella pneumophila, Brucella spp., Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii,
Also gram-positive aerobic bacteria are sensitive to ciprofloxacin: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae).
Aktivenvotnosheniya Bacillus anthracis.
The majority of the stafilokokk steady against Methicillinum, rezistentna and to ciprofloxacin. Sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) - moderated (for their suppression high concentration are required).
To rezistentna drug: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. It is not effective concerning Treponema pallidum.
Resistance develops extremely slowly as, on the one hand, after effect of ciprofloxacin there is practically no persistent microorganism left, and with another - bacterial cells have no enzymes inactivating it.
The lactulose which is Ekotsifol's part as a bifidogenny factor is synthetic disaccharide which molecule consists of the remains of a galactose and fructose. Lactulose in a stomach and upper parts of intestines is not soaked up and not hydrolyzed. Ekotsifola who is released from tablets lactulose as substrate is fermented by normal microflora of a large intestine, stimulating growth of bifidobacteria and lactobacilli. As a result of hydrolysis of lactulose in a large intestine organic acids - milk, acetic and ant, suppressing growth of pathogenic microorganisms and reducing thereof products of nitrogen-containing toxic substances are formed.
Thus, lactulose as a part of Ekotsifol reduces the damaging action of an antibiotic on the normal intestinal microflora and risks of side effects connected with disbioza.

Pharmacokinetics. At oral administration it is quickly and rather fully soaked up from digestive tract (preferential in 12-perstny and a jejunum). Meal slows down absorption, but does not change the maximum concentration (Cmax) and bioavailability. Bioavailability - 50-85%, distribution volume - 2-3,5 l/kg, communication with proteins of plasma - 20-40%. Time of achievement of the maximum concentration (TCmax) - 60-90 min., the maximum concentration linearly depends on the size of the accepted dose and makes at doses 250, 500, 750 both 1000 mg respectively 1, 2, 2.4, 4.3 and 5.4 mkg/ml. In 12 h after intake of 250, 500 and 750 mg concentration of drug in plasma decreases to 0.1, 0.2 and 0.4 mkg/ml respectively.
It is well distributed in body tissues (excepting the fabric rich with fats, for example nervous tissue). Concentration in fabrics is 2-12 times higher, than in plasma. Therapeutic concentration are reached in saliva, almonds, a liver, a gall bladder, bile, intestines, abdominal organs and a small pelvis (an endometria, fallopian pipes and ovaries, a uterus), semen, prostate gland tissue, kidneys and urinary bodies, pulmonary fabric, a bronchial secret, a bone tissue, muscles, synovial fluid and joint cartilages, peritoneal liquid, skin. Gets into cerebrospinal fluid in a small amount where its concentration in the absence of an inflammation of a meninx makes 6-10% of that in blood serum, and at inflamed - 14-37%. Ciprofloxacin well gets also into eye liquid, a pleura, a peritoneum, a lymph, through a placenta. Concentration of ciprofloxacin in neutrophils of blood is 2-7 times higher, than in blood serum.
It is metabolized in a liver (15-30%) with formation of low-active metabolites (diethylciprofloxacin, sulfociprofloxacin, oxociprofloxacin, formylciprofloxacin).
Elimination half-life - about 4 h, at a chronic renal failure - to 12 h. Other part - through digestive tract is removed generally by kidneys by canalicular filtering and canalicular secretion in not changed look (40-50%) and in the form of metabolites (15%). A small amount is removed with breast milk.
Renal clearance - 3-5 ml/min.; the general clearance - 8-10 ml/min.
At a chronic renal failure (the clearance of creatinine is higher than 20 ml/min.) the percent of the ciprofloxacin removed through kidneys decreases, but cumulation in an organism does not happen owing to compensatory increase in metabolism of ciprofloxacin of removal through digestive tract.
The lactulose which is Ekotsifol's part does not exert impact on the key pharmacokinetic parameters characterizing bioavailability of a tsirofloksatsin.

Indications to use:

The infectious and inflammatory diseases caused by sensitive microorganisms:
— diseases of the lower respiratory tracts (acute and chronic (in an aggravation stage) bronchitis, pneumonia, a bronchoectatic disease, infectious complications of a mucoviscidosis);
— infections of ENT organs (acute sinusitis);
— infections of kidneys and urinary tract (cystitis, pyelonephritis);
— the complicated intraabdominal infections (in a combination with metronidazole);
— chronic bacterial prostatitis;
— uncomplicated gonorrhea;
— typhoid, campilobacteriosis, shigellosis, diarrhea of "travelers";
— the infections of skin and soft tissues (infected ulcers, wounds, burns, abscesses, phlegmon);
— bones and joints (osteomyelitis, septic arthritis);
— infections against the background of the immunodeficiency (arising at treatment by immunodepressive medicines or at patients with a neutropenia);
— prevention and treatment of a pulmonary form of a malignant anthrax.

Children:
— therapy of the complications caused by Pseudomonas aeruginosa in children with a mucoviscidosis of easy from 5 to 17 years;
— prevention and treatment of a pulmonary form of a malignant anthrax (Bacillus anthracis infection).

Route of administration and doses:

Inside. Tablets should be swallowed entirely with a small amount of liquid after food. At reception of a tablet on an empty stomach active agent is soaked up quicker.
At lower respiratory tract infections of easy and average degree - 0.5 g 2 times/days, at a heavy current - 0.75 g 2 times/days. A course of treatment - 7-14 days.
At acute sinusitis - on 0.5 g 2 times/days. A course of treatment - 10 days.
At an infection of skin and soft tissues of easy and average degree - 0.5 g 2 times/days, at a heavy current - 0.75 g 2 times/days. A course of treatment - 7-14 days.
At infections of bones and joints - easy and average degree - 0.5 g 2 times/days, at a heavy current - 0.75 g 2 times/days. A course of treatment - to 4-6 weeks.
At infections of urinary tract - on 0.25-0.5 g 2 times/days; a course of treatment - 7-14 days, at uncomplicated cystitis at women - 3 days.
At chronic bacterial prostatitis - on 0.5 g 2 times/days, a course of treatment - 28 days.
At uncomplicated gonorrhea - 0.25-0.5 g once.
Acute intestinal infections (salmonellosis, shigellosis, campilobacteriosis, etc.) - on 0.5 g 2 times/days, a course of treatment - 5-7 days.
At a typhoid - on 0.5 g 2 times/days; a course of treatment - 10 days.
At the complicated intraabdominal infections - on 0.5 g each 12 h within 7-14 days.
For prevention and treatment of a pulmonary form of a malignant anthrax - on 0.5 g 2 times/days within 60 days.
At patients with an immunodeficiency treatment is appointed depending on weight of an infection and a type of the activator. An antibioticotherapia is carried out during the entire period of a neutropenia.

In pediatrics:
at treatment of the complications caused by Pseudomonas aeruginosa children with a mucoviscidosis of lungs have from 5 to 17 years - 20 mg/kg of 2 times/days (the maximum dose of 1.5 g). Treatment duration - 10-14 days.
At a pulmonary form of a malignant anthrax (prevention and treatment) - 15 mg/kg of 2 times/days. The maximum single dose - 0.5 g, daily - 1 g. The general duration of reception of ciprofloxacin - 60 days.
Chronic renal failure: at the clearance of creatinine (CC) more than 50 ml/min. of dose adjustment are not required; at KK of 30-50 ml/min. - 0.25-0.5 each 12 h; at KK of 5-29 ml/min. - 0.25-0.5 g each 18 h. If to the patient the hemodialysis or peritoneal dialysis - 0.25-0.5 g / is carried out, it is necessary to accept drug after the hemodialysis session.

Features of use:

Ciprofloxacin is not choice drug at the suspect or the established pneumonia caused by Streptococcus pneumoniae.

In order to avoid development of a crystalluria exceeding of the recommended daily dose is inadmissible, also sufficient consumption of liquid and maintenance of acid reaction of urine is necessary.

During treatment it is necessary to abstain from occupations potentially dangerous types of activity requiring special attention and speed of mental and motor reactions.

The patient with epilepsy, attacks of spasms in the anamnesis, vascular diseases and organic lesions of a brain in connection with threat of development of side reactions from the central nervous system it is necessary to appoint ciprofloxacin only according to "vital" indications.

At emergence in time or after treatment by ciprofloxacin of heavy and long diarrhea it is necessary to exclude the diagnosis of pseudomembranous colitis which demands immediate drug withdrawal and purpose of the corresponding treatment.

When developing pains in sinews or at emergence of the first symptoms of a tendovaginitis treatment should be stopped because separate cases of an inflammation and even a rupture of sinews are described during treatment of a ftorkhinolonama.

During treatment by ciprofloxacin it is necessary to avoid UF-radiation (including contact with direct sunshine).

Side effects:

From the alimentary system: nausea, diarrhea, vomiting, abdominal pains, a meteorism, anorexia, cholestatic jaundice (especially at patients with the postponed liver diseases), hepatitis, гепатонекроз.
From the central nervous system: dizziness, a headache, increased fatigue, feeling of alarm, a tremor, sleeplessness, "dreadful" dreams, a peripheral paralgeziya (anomaly of perception of feeling of pain), perspiration, increase in intracranial pressure, confusion of consciousness, a depression, hallucinations, and also other manifestations of the psychotic reactions (which are occasionally progressing to states in which the patient can do himself harm), migraine, faints, thrombosis of cerebral arteries.
From sense bodys: disturbances of taste and sense of smell, vision disorder (diplopia, change of color perception), sonitus, decrease in hearing.
From cardiovascular system: tachycardia, disturbances of a cordial rhythm, lowering of arterial pressure.
From circulatory system: leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolitic anemia.
Laboratory indicators: prothrombinopenia, increase in activity of "hepatic" transaminases and alkaline phosphatase, giperkreatininemiya, hyperbilirubinemia, hyperglycemia.
From an urinary system: a hamaturia, a crystalluria (first of all at alkalinuria and a hypouresis), a glomerulonephritis, a dysuria, a polyuria, an ischuria, an albuminuria, urethral bleedings, decrease in azotovydelitelny function of kidneys, intersticial nephrite.
Allergic reactions: a skin itch, a small tortoiseshell, blistering, followed by bleedings, and emergence of the small small knots forming crusts, medicinal fever, dot hemorrhages on skin (petechia), a face edema or throats, short wind, an eosinophilia, a vasculitis, a knotty erythema, an exudative multiformny erythema, Stephens-Johnson's syndrome (a malignant exudative erythema), a toxic epidermal necrolysis (Lyell's disease).
From a musculoskeletal system: arthralgia, arthritis, tendovaginitis, ruptures of sinews, mialgiya.
Others: the general weakness, the raised photosensitivity, superinfections (candidiasis, pseudomembranous colitis), rushes of blood to the person.

Interaction with other medicines:

Owing to decrease of the activity of processes of a microsomal oxidation in hepatocytes increases concentration and extends a theophylline elimination half-life (and other xanthines, for example caffeine), peroral hypoglycemic medicines, indirect anticoagulants, promotes decrease in a prothrombin ratio.

At a combination to other antimicrobic medicines (beta лактамные antibiotics, aminoglycosides, clindamycin, metronidazole) a synergism is usually observed; it can successfully be applied in a combination with azlotsilliny and a ceftazidime at the infections caused by Pseudomonas spp.; with mezlotsilliny, azlotsilliny, etc. beta лактамными antibiotics - at streptococcal infections; with izoksazolilpenitsillina and Vancomycinum - at staphylococcal infections; with metronidazole and clindamycin - at mephitic gangrenes.

Strengthens nephrotoxic effect of cyclosporine, increase in serumal creatinine is noted, at such patients control of this indicator 2 times a week is necessary.

At a concomitant use strengthens effect of indirect anticoagulants.

Oral administration together with ferriferous medicines, sukralfaty and the antiacid medicines containing salts of magnesium, calcium and aluminum leads to decrease in absorption of ciprofloxacin therefore it is necessary to appoint it for 1-2 h to or in 4 h after reception of the above-stated medicines.

Non-steroidal anti-inflammatory drugs (excepting acetylsalicylic acid) increase risk of development of spasms.

Ftorkhinolona form chelate connections with ions of magnesium and aluminum of buffer system of a dosage form of a didanozin that sharply reduces absorption of antibiotics therefore ciprofloxacin is accepted in 2 hours prior to reception of a didanozin or in 2 hours after reception of the specified drug

Metoclopramidum accelerates absorption that leads to reduction of time of achievement of its maximum concentration.

Combined use of uricosuric medicines leads to removal delay (up to 50%) and increase in plasma concentration of ciprofloxacin.

Increases the maximum concentration by 7 times (from 4 to 21 times) and the area under a curve "concentration time" by 10 times (from 6 to 24 times) of a tizanidin that increases risk of the expressed lowering of arterial pressure and drowsiness.

Contraindications:

— hypersensitivity;
— a concomitant use with tizanidiny (risk of the expressed lowering of arterial pressure, drowsiness);
— age up to 18 years (before completion of process of formation of a skeleton, except therapy of the complications caused by Pseudomonas aeruginosa in children with a mucoviscidosis of easy from 5 to 17 years; prevention and treatment of a pulmonary form of a malignant anthrax);
— pregnancy;
— lactation period.

With care
The expressed atherosclerosis of vessels of a brain, disturbance of cerebral circulation, mental diseases, epilepsy, the expressed renal and/or liver failure, advanced age.

Use of drug EKOTsIFOL at pregnancy and feeding by a breast
It is prohibited to use at pregnancy during breastfeeding.

Use at abnormal liver functions
With care to appoint at the expressed liver failure.

Use at renal failures
With care to appoint at the expressed renal failure.

Use for elderly patients
To apply with care at advanced age.

Use for children
It is contraindicated at children's age, except therapy of the complications caused by Pseudomonas aeruginosa in children with a mucoviscidosis of easy from 5 to 17 years.

Overdose:

The special antidote is unknown. It is necessary to control carefully a condition of the patient, to make a gastric lavage, to carry out usual measures of acute management, to provide sufficient intake of liquid. By means of haemo - or peritoneal dialysis the amount of drug can be removed only insignificant (less than 10%).

Storage conditions:

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

Issue conditions:

According to the recipe

Packaging:

Tablets, покр. film cover, 500 mg: 10 pieces.