Урсокапс

General characteristics. Structure:

Active ingredient: 250 mg of acid ursodeoksikholevy.

Excipients: lecithin (V-10 Solkas), beeswax, sunflower oil.

Structure of a cover of the capsule: gelatin, глицерол, the water purified, methylparahydroxybenzoate, titanium dioxide, dye a sunset yellow (E110).

Gepatoprotektor, the drug promoting dissolution of cholesteric gallstones. Renders hepatoprotective, cholagogue, cholelitholytic, gipokholesterinemichesky, hypolipidemic and some immunomodulatory action.

Pharmacological properties:

Pharmacodynamics. Renders gepatoprotektivny, cholagogue, cholelitholytic, gipokholesterinemichesky, hypolipidemic and some immunomodulatory action.

It is built in a hepatocyte membrane, stabilizes its structure and protects a hepatocyte from the damaging effect of salts of bile acids, reducing, thus, cytotoxic effect. At a cholestasia activates Ca2+-dependent alphaprotease and stimulates an exocytosis, reduces concentration of toxic bile acids (chenodesoxycholic, lithocholic, deoxycholic, etc.) which concentration at patients with chronic diseases of a liver are overestimated.

Having high polarity, acid ursodeoksikholevy forms the nontoxic mixed micelles with non-polar (toxic) bile acids that reduces ability of a gastric reflyuktat to damage cellular membranes at a biliary reflyuksgastrit and a reflyuksezofagita. Besides, acid ursodeoksikholevy forms the double molecules capable to be included cellular membranes (hepatocytes, holangiotsit, GIT epithelial cells), to stabilize them and to do unreceptive to action of cytotoxic micelles – the cytoprotective, gepatoprotektivny effect.

Reduces a bile saturation cholesterol due to oppression of its absorption in intestines, suppression of synthesis in a liver and decreases in secretion in bile; increases solubility of cholesterol in bile, forming with it liquid crystals; reduces a litogenny index of bile. Dissolution of cholesteric gallstones (a consequence of change of a ratio cholesterol / bile acids in bile) and the prevention of formation of new concrements (result of reduction of content in cholesterol bile) - litolitichesky effect is result.

Induces the cholepoiesis rich with bicarbonates that leads to increase in a passage of bile and stimulates removal of toxic bile acids through intestines that promotes permission of an intra hepatic cholestasia - anti-cholestatic effect.

Immunomodulatory action is caused by oppression of an expression of HLA antigens on membranes of hepatocytes and holangiotsit, decrease of the activity of immunocompetent immunoglobulins (first of all Ig M), normalization of a natural killerny lymphocyte activity, influence on education interleykina-2, reduction of quantity of eosinophils and др

Authentically progressing of fibrosis at patients with primary biliary cirrhosis, a mucoviscidosis and alcoholic steatogepatit – antifibrolitichesky effect detains. Reduces risk of development of a varicosity of a gullet.

Acid ursodeoksikholevy slows down processes of a senilism and death of cells (hepatocytes, holangiotsit, etc.) - anti-apoptotic effect. Slows down growth of cells of a colorectal cancer (antineoplastic action concerning a colon cancer).

Pharmacokinetics. At intake it is absorbed in a small bowel due to passive diffusion, and in an ileal gut by means of active transport. Cmax is reached in 1-3 h. Linkng with proteins high (at healthy volunteers at least 70% of not conjugated acid ursodeoksikholevy are connected with proteins

At reception in a single dose of 500 mg concentration in blood serum in 30, 60 and 90 min. makes 3,8; 5,5 and 3,7 µmol/l respectively. At systematic reception acid ursodeoksikholevy becomes the main bile acid of blood serum (48% of the general contents of bile acids).
The therapeutic effect depends on concentration of acid ursodeoksikholevy in bile; against the background of therapy there is a dozozavisimy increase in its share in a bullet of bile acids up to 50-75% (at daily doses of 10-20 mg/kg). Joins in system of gastrointestinal circulation. In a liver acid ursodeoksikholevy contacts glycine and taurine; the formed conjugates cosecrete in bile.

Passes through a placental barrier. It is removed preferential (50-70%) through intestines, very small quantity (less than 1%) – with urine. The insignificant amount of not soaked up acid ursodeoksikholevy in a large intestine is exposed to splitting by bacteria (7 dehydroxylation) to lithocholic acid which is partially soaked up from a large intestine, is sulphated in a liver and quickly removed with excrements in the form of sulfotilkholilglitsinovy or sulfotilkholiltaurinovy conjugates. A part of lithocholic acid at enterogepatichesky circulation gets into a liver and retransformirutsya in heno-and the ursodeoksikho-left acids again.

Indications to use:

- patients with high operational risk and at patients have a dissolution of bilious cholesteric stones after a lithotripsy. A condition of success of treatment is the functioning gall bladder and presence of pure radiotransparantny cholesteric stones which diameter does not exceed 2 cm;
- primary biliary cirrhosis of I and II stages;
- primary sclerosing cholangitis;
- hepatitis (chronic, active including atypical forms chronic autoimmune, chronic and acute virus);
- not alcoholic steatogepatit;
- toxic (including alcoholic, medicinal) damages of a liver;
- mucoviscidosis (cystous fibrosis of a liver);
- biliary reflux gastritis;
- biliary reflux esophagitis;
- biliary dyspepsia;
- dyskinesia of bilious ways;
- cholestatic diseases of a liver at children (including an atresia of bilious channels);
- a cholestasia after transplantation of a liver;
- chronic opisthorchosis;
- prevention of a colon cancer at patients with high risk of its development (for example, at ulcer colitis);
- prevention of formation of bilious concrements at patients with obesity during bystry loss of weight.

Route of administration and doses:

Capsules of Ursokaps accept inside, irrespective of meal, washing down with enough liquid. The mode of dosing and duration of treatment are established individually and weights of a condition of the patient depend on indications.

Average dosage of 8-10 mg/kg/days within 6-12 months

Cholelithiasis, reflux gastritis: 1 time a day before going to bed.

Chronic diseases of a liver, cholesteric gallstones: continuously for a long time (from several months to several years) in a daily dose from 10 mg/kg to 12-15 mg/kg (2-5 капс.). Reception duration for dissolution of stones – before full dissolution + 3 months for prevention of a recurrence of a lithogenesis.

Biliary reflux gastritis and biliary reflux esophagitis: 250 mg/days (1 capsule); a course of treatment from 10-14 days to 2 years.

Primary biliary cirrhosis: 8-15 mg/kg/days (if necessary – to 20 mg/kg) within 6-24 months (up to several years).

Primary sclerosing cholangitis: 12-15 mg/kg/days (to 20 mg) within 6-24 months (up to several years).

Mucoviscidosis: to 20-30 mg/kg/days within 6-24 months and more

Toxic and alcoholic damages of a liver: 10-15 mg/kg/days within 6-12 months and more.

Features of use:

At cholelithiasis control of efficiency of treatment is exercised each 6 months by carrying out radiological and ultrasound examination of biliary tract for the purpose of prevention of a recurrence of a cholelithiasis.

Positive results can be received only in the presence of purely cholesteric (X-ray negative) gallstones no more than 15-20 mm in size, at the kept function of a gall bladder and passability vesical and the general bilious channels.

At long (more than 1 month) treatment it is necessary to carry out monthly biochemical analysis of blood for definition of activity of hepatic transaminases, an alkaline phosphatase, gamma глутамилтрансферазы and bilirubin (especially to the first 3 months of therapy). At preservation of the raised indicators drug should be cancelled.

After full dissolution of concrements it is recommended to continue use within, at least, 3 months to promote dissolution of the remains of concrements which sizes are too small for their detection.

If within 6-12 months after the beginning of therapy of partial dissolution of concrements did not occur, it is improbable that treatment will be effective. Detection during treatment of not visualized gall bladder is the certificate that full dissolution of concrements did not happen, and treatment should be stopped.

During treatment of the woman of childbearing age by Ursokaps have to apply non-hormonal methods of contraception or contraceptives with the low content of estrogen.

Does not influence speed of response during the driving of cars and management of the automated means.

Side effects:

Урсокапс it is rather well transferred by patients. There can seldom be diarrhea or a lock, nausea, vomiting, pain in epigastric area and the right hypochondrium, calcination of gallstones, increase in activity of hepatic transaminases, an exacerbation of earlier being available psoriasis, allergic reactions (rashes, a skin itch), dizziness, allergic reactions.

At treatment of primary biliary cirrhosis the passing decompensation of cirrhosis which disappears after drug withdrawal can be observed.

In case of any unusual reactions it is necessary to stop administration of drug and to consult with the doctor.

Interaction with other medicines:

Colestyraminum, cholesterol and antacids containing aluminum hydroxide connect acid ursodeoksikholevy in intestines, reduce its absorption and weaken efficiency. In case of need simultaneous treatment above-mentioned drugs recommend to apply them for 2 h to or after Ursokaps's reception.

Hypolipidemic medicines (especially Clofibratum), are oestrogenic, Neomycinum, progestins can increase bile saturation by cholesterol and reduce ability of acid ursodeoksikholevy to dissolve cholesteric bilious concrements.

Урсокапс can increase absorption of cyclosporine in intestines. Therefore it is necessary to control the level of cyclosporine at the people who are at the same time accepting this drug and to adjust its doses.

Contraindications:

- hypersensitivity;

- X-ray positive (with the high content of calcium) gallstones;

- acute inflammatory diseases of a gall bladder, bilious channels and intestines, disease Krone;

- nonfunctioning gall bladder;

- full obstruction of bilious ways;

- cirrhosis in a decompensation stage;

- the expressed renal failures, a liver, a pancreas;

- желче - gastrointestinal fistula;

- acute cholecystitis;

- acute cholangitis;

- pregnancy;

- lactation period;

- children's age up to 6 years;

- frequent biliary gripes.

Overdose:

Cases of overdose of ursodezoksikholevy acid are not known.

Storage conditions:

Drug should be stored in the unavailable to children, protected from moisture and light place at a temperature from 15 °C to 25 °C. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

On 10 capsules in blister strip packagings, on 5 strip packagings in cardboard boxes.