Ursosan® (Ursosan®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Dosage form: & nbspcapsules
Composition:

Each capsule contains:

active substance - 250 mg of ursodeoxycholic acid.

Excipients - corn starch, corn starch pregelatinized, silicon dioxide colloid, magnesium stearate.

Capsule shell: gelatin, titanium dioxide.

Description:

White, hard, opaque gelatin capsules № 0.

Contents of the capsules: white or almost white powder, or white or almost white powder with slices of mass, or white or almost white pressed powder, disintegrating upon pressing.

Pharmacotherapeutic group:Hepatoprotective agent
Pharmacodynamics:

Hepatoprotective agent, also has choleretic, cholelitholytic, hypolipidemic, hypocholesterolemic and some immunomodulating action.

Possessing high polar properties, ursodeoxycholic acid (UDCA) is embedded in the membrane of the hepatocyte, cholangiocyte and epitheliocyte of the gastrointestinal tract, stabilizes its structure and protects the cell from damaging effects of salts of toxic bile acids, thus reducing their cytotoxic effect. Forms non-toxic mixed micelles with apolar (toxic) bile acids, which reduces the ability of gastric reflux to damage cell membranes with biliary reflux gastritis and reflux esophagitis.Reducing concentration and stimulating choleresis, rich in bicarbonates, UDCA effectively contributes to the resolution of intrahepatic cholestasis. When cholestasis activates Ca2+-dependent alpha protease and stimulates exocytosis, reduces the concentration of toxic bile acids (chenodeoxycholic, lithocholic, deoxycholic, etc.), whose concentrations in patients with chronic liver diseases are increased.

Competitive reduces the absorption of lipophilic bile acids in the intestine, increases their "Fractional" turnover under enterohepatic circulation cholepoiesis induces, promotes the passage of bile and excretion of toxic bile acids across the gut. Reduces the saturation of bile with cholesterol due to inhibition of its absorption in the intestine, suppression of synthesis in the liver and a decrease in secretion in bile; increases the solubility of cholesterol in bile, forming with it liquid crystals; reduces the lithogenic index of bile, increases the concentration of bile acids in it, causes an increase in gastric and pancreatic secretion, increases lipase activity, and has a hypoglycemic effect. Causes partial or complete dissolution of cholesterol gallstones, reduces the saturation of bile with cholesterol, which contributes to its mobilization from gallstones.The result is the dissolution of cholesterol gallstones and the prevention of the formation of new concrements. Immunomodulating effect is due to inhibition of histocompatibility antigen expression - HLA-1 - on membranes of hepatocytes and HLA-2 - on cholangiocytes, normalization of the natural killer activity of lymphocytes, the formation of interleukin-2, a decrease in the number of eosinophils, suppression of immunocompetent immunoglobulins (Ig), Firstly - IgM. Delays the progression of fibrosis. Regulates the processes of apoptosis of hepatocytes, cholangiocytes and epitheliocytes of the gastrointestinal tract.

Pharmacokinetics:

UDCA is absorbed in the small intestine due to passive diffusion (about 90%), and in the ileum through active transport. The maximum concentration in the blood plasma (CmOh) with ingestion of 50 mg after 30, 60, 90 minutes - 3.8 mmol / l, 5.5 mmol / l and 3.7 mmol / l, respectively. Time to reach the maximum concentration in the plasma (TCmOh) is achieved in 1-3 hours. The connection with plasma proteins is high - up to 96-99%. Penetrates through the placental barrier. With the systematic administration of the drug UDCA becomes the main bile acid in the blood serum.Metabolised in the liver (clearance at the "primary passage" through the liver) into taurine and glycine conjugates. The resulting conjugates are secreted in bile. About 50-70% of the total dose of the drug is excreted with bile. A small amount of unsweetened UDCA enters the large intestine, where it undergoes cleavage by bacteria (7-dehydroxylation); the resulting lithocholic acid is partially absorbed from the colon but is sulfated in the liver and is rapidly excreted as a sulfolithocholylglycine or sulfolithocholyltaurine conjugate.

Indications:

- Uncomplicated cholelithiasis (SCI): biliary sludge; dissolution of cholesterol gallstones with a functioning gallbladder; prevention of stone recurrence after cholecystectomy

- Chronic hepatitis of various genesis (toxic, medicinal, etc.)

- Cholestatic diseases of the liver of various genesis, including primary biliary cirrhosis, primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis)

- Non-alcoholic fatty liver disease, including non-alcoholic steatohepatitis

- Alcoholic liver disease

- Viral hepatitis chronic

- Dyskinesia of the biliary tract

- Biliary reflux gastritis and reflux esophagitis

Contraindications:

Hypersensitivity, x-ray positive (with a high calcium content) gallstones, a dysfunctional gallbladder, marked violations of the kidneys, liver, pancreas, cirrhosis in the decompensation stage, acute infectious and inflammatory diseases of the biliary tract.

Ursodeoxycholic acid has no age limitation in use, but children under 3 years of age are not recommended to use the drug in this dosage form.

Pregnancy and lactation:

The use of UDCA during pregnancy is possible only if the expected benefit for the mother exceeds the potential risk to the fetus. Data on the isolation of ursodeoxycholic acid with breast milk are currently not available. If UDCA is necessary in the lactation period, the question of stopping breastfeeding should be addressed.

Dosing and Administration:

Inside, squeezed a little water.

To dissolve cholesterol gallstones, the average daily dose of the drug is 10-15 mg / kg. The course of treatment is 6-12 months and more until the stones are completely dissolved. With LCD, the whole daily dose of the drug is taken once for the night.

To prevent the re-formation of stones, the use of the drug is recommended for several months after the dissolution of the stones.

After cholecystectomy for the prevention of recurrent cholelithiasis, 250 mg twice a day for several months.

In chronic hepatitis of various genesis (toxic, medicinal, etc.), chronic viral hepatitis, non-alcoholic fatty liver disease, including non-alcoholic steatohepatitis, alcoholic liver disease, the average daily dose is 10-15 mg / kg in 2-3 doses. The duration of therapy is 6-12 months or more.

With cholestatic liver diseases of various genesis, including: primary biliary cirrhosis, primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis), the average daily dose is 12-15 mg / kg; if necessary daily dose may be increased to 20-30 mg / kg in 2-3 doses. Duration therapy ranges from 6 months to several years.

When dyskinesia of the bile ducts is hypokinetic, the average daily dose is 10 mg / kg in 2 divided doses for 2 weeks to 2 months. If necessary, the course of treatment is recommended to be repeated.

With biliary reflux gastritis and reflux esophagitis - 250 mg per day, before bedtime. The course of treatment - from 10-14 days to 6 months, if necessary - up to 2 years.

Calculation of the daily number of capsules depending on the patient's body weight and the recommended dose of the drug per 1 kg of body weight (mg / kg / day)

body mass

10 mg / kg / day

12 mg / kg / day

15 mg / kg / day

20 mg / kg / day

30 mg / kg / day

19-25 kg

1 caps

1 caps

2 caps

2 caps

3 caps

26-30 kg

1 caps

1 caps

2 caps

2 caps

4 caps

31-35 kg

1 caps

2 caps

2 caps

3 caps

4 caps

36-40 kg

2 caps

2 caps

2 caps

3 caps

5 caps

41-45 kg

2 caps

2 caps

3 caps

4 caps

5 caps

45-50 kg

2 caps

2 caps

3 caps

4 caps

6 caps

51-55 kg

2 caps

3 caps

3 caps

4 caps

7 caps

56-60 kg

2 caps

3 caps

4 caps

5 caps

7 caps

61-65 kg

3 caps

3 caps

4 caps

5 caps

8 caps

66-70 kg

3 caps

3 caps

4 caps

6 caps

8 caps

71-75 kg

3 caps

4 caps

5 caps

6 caps

9 caps

76-80 kg

3 caps

4 caps

5 caps

6 caps

10 caps

81-85 kg

3 caps

4 caps

5 caps

7 caps

10 caps

86-90 kg

4 caps

4 caps

5 caps

7 caps

11 caps

91-95 kg

4 caps

5 caps

6 caps

8 caps

11 caps

96-100 kg

4 caps

5 caps

6 caps

8 caps

12 caps

101-105 kg

4 caps

5 caps

6 caps

8 caps

13 caps

105-110 kg

4 caps

5 caps

7 caps

9 caps

13 caps
Side effects:

Diarrhea (can be dose-dependent).

Rarely, calcification of gallstones, transitory (transient) increase in the activity of "liver" transaminases, nausea, vomiting, abdominal pain, allergic reactions.

Overdose:

Cases of drug overdose are not known.

Interaction:

Antacids containing aluminum and ion-exchange resins (colestramine), reduce absorption. Lipid-lowering drugs (especially clofibrate), estrogens, neomycin or progestins increase bile saturation with cholesterol and may decrease the ability to dissolve cholesterol bile stones.

Special instructions:

When taking the drug for the purpose of dissolution of gallstones, it is necessary to observe the following conditions: the stones must be cholesterol (X-ray negative), their size should not exceed 15-20 mm, the gallbladder should remain functional and should be filled with stones no more than half, the permeability of the cystic and of the common bile duct should be preserved.

With prolonged (more than 1 month) taking the drug to dissolve gallstones,every 4 weeks in the first 3 months of treatment, then - every 3 months to conduct a biochemical blood test to determine the activity of "liver" transaminases. Control of the effectiveness of treatment should be carried out every 6 months according to ultrasound examination of the biliary tract. After complete dissolution of the stones, it is recommended to continue the use of the drug for 3 months in order to promote the dissolution of stone remains, the sizes of which are too small for their detection and for the prevention of stone recurrence.

Form release / dosage:Capsules, 250 mg.
Packaging:

10 capsules per blister; 1, 5 or 10 blisters in a cardboard box together with instructions for use.

Storage conditions:

In a dry, dark place at a temperature of 15-25 ° C.

Keep out of the reach of children!

Shelf life:

4 years. Do not use after the expiration date!

Terms of leave from pharmacies:On prescription
Registration number:П N016302 / 01
Date of registration:26.02.2010 / 26.08.2010
Expiration Date:Unlimited
The owner of the registration certificate:PRO.MED.CS Prague as.PRO.MED.CS Prague as. Czech Republic
Manufacturer: & nbsp
Representation: & nbspPRO.MED.CS Prague as. PRO.MED.CS Prague as. Czech Republic
Information update date: & nbsp13.07.2016
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