Ursosan 250 mg

Active substance: 

ursodeoxycholic acid - 250 mg.

Excipients: 

corn starch - 49 mg;

pregelatinized corn starch - 24 mg;

colloidal silicon dioxide - 5 mg;

magnesium stearate - 3.65 mg.

Capsule shell:

gelatin - 98 mg;

titanium dioxide - 2 mg.

Hepatoprotector. It also has choleretic, cholelitholytic, hypolipidemic, hypocholesterolemic and some immunomodulatory effects.

With its high polar properties, ursodeoxycholic acid forms non-toxic mixed micelles with apolar (toxic) bile acids, which reduces the ability of gastric reflux to damage cell membranes in biliary reflux gastritis and reflux esophagitis. In addition, ursodeoxycholic acid forms double molecules that can be incorporated into the cell membranes of hepatocytes, cholangiocytes, gastrointestinal epithelial cells, stabilize them and make them immune to cytotoxic micelles.

By reducing the concentration of bile acids toxic to hepatocytes and stimulating bicarbonate-rich choleresis, ursodeoxycholic acid effectively helps resolve intrahepatic cholestasis. Reduces the saturation of bile with cholesterol due to inhibition of its absorption in the intestine, suppression of synthesis in the liver and lower secretion in bile; increases the solubility of cholesterol in bile, forming liquid crystals with it; reduces the lithogenic bile index. The result is the dissolution of cholesterol gallstones and the prevention of the formation of new calculi.

The immunomodulatory effect is due to inhibition of the expression of HLA-1 antigens on the membranes of hepatocytes and HLA-2 on cholangiocytes, normalization of the natural killer activity of lymphocytes, etc. Reliably delays the progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis and alcoholic steatohepat; reduces the risk of varicose veins of the esophagus. Ursodeoxycholic acid slows down the processes of premature aging and cell death (hepatocytes, cholangiocytes).

Pharmacokinetics

Suction and distribution

Ursodeoxycholic acid is absorbed from the small intestine due to passive diffusion (about 90%), and in the ileum through active transport. In this case, the concentration of ursodeoxycholic acid when taking the drug inside at a dose of 50 mg after 30, 60, 90 minutes is 3.8 mmol / L, 5.5 mmol / L and 3.7 mmol / L, respectively. Cmax is reached in 1-3 hours.

Plasma protein binding is high - up to 96-99%. Penetrates through the placental barrier. With the systematic administration of Ursosan, ursodeoxycholic acid becomes the main bile acid in the blood serum and makes up about 48% of the total amount of bile acids in the blood. The therapeutic effect of the drug depends on the concentration of ursodeoxycholic acid in bile.

Metabolism and excretion

It is metabolized in the liver (clearance during the initial passage through the liver) into taurine and glycine conjugates. The resulting conjugates are secreted into the bile. About 50-70% of the total dose of the drug is excreted in the bile. A small amount of non-absorbable ursodeoxycholic acid enters the colon, where it is digested by bacteria (7-dehydroxylation); the resulting lithocholic acid is partially absorbed from the colon, but sulfates in the liver and is rapidly excreted in the form of a sulfolithocholylglycine or sulfolithocholyltaurin conjugate.

The use of ursodeoxycholic acid in pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus (adequate, strictly controlled studies of the use of ursodeoxycholic acid in pregnant women have not been conducted).

Data on the allocation of ursodeoxycholic acid with breast milk are currently not available. If it is necessary to use ursodeoxycholic acid during lactation, the issue of stopping breastfeeding should be addressed.

• X-ray positive (high calcium) gallstones;
• non-functioning gall bladder;
• biliary and gastrointestinal fistula;
• acute cholecystitis;
• acute cholangitis;
• decompensated liver cirrhosis;
• liver failure;
• renal failure;
• obstruction of the biliary tract;
• acute infectious diseases of the gallbladder and bile ducts;
• empyema of the gallbladder;
• hypersensitivity to the components of the drug.

Ursosan is used with caution: in children aged 2 to 4 years, since it is possible to swallow capsules, although ursodeoxycholic acid has no age restrictions in use.

Diarrhea (may be dose dependent).

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

Inside, washed down with a small amount of water.

For the dissolution of cholesterol gallstones, the average daily dose of the drug is 10-15 mg / kg. The course of treatment is 6-12 months or more until the stones completely dissolve. In gallstone disease, the entire daily dose of the drug is taken once at night.

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

After cholecystectomy for the prevention of re-cholelithiasis - 250 mg 2 times a day for several months.

With chronic hepatitis of various origins (toxic, drug), 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 diseases of the liver of various origins, including primary biliary cirrhosis, primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis), the average daily dose is 12-15 mg / kg; if necessary, the average daily dose can be increased to 20-30 mg / kg in 2-3 doses. The duration of therapy is from 6 months to several years.

With biliary dyskinesia according to the hypokinetic type, the average daily dose is 10 mg / kg in 2 divided doses for 2 weeks to 2 months. If necessary, the treatment is recommended to be repeated.

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

Cases of an overdose of ursodeoxycholic acid are not known.

When taking the drug in order to dissolve gallstones, the following conditions must be met: the stones must be cholesterol (X-ray negative), their size should not exceed 15–20 mm, the gallbladder should remain functioning and be filled with no more than half stones, patency of the gallbladder and general gall the duct must be preserved.

With long-term (more than 1 month) administration of the drug every 4 weeks in the first 3 months of treatment, in the future - every 3 months a blood chemistry test should be performed to determine the activity of hepatic transaminases. Monitoring the effectiveness of treatment should be carried out every 6 months according to ultrasound of the biliary tract.

After complete dissolution of the stones, it is recommended to continue using the drug for at least 3 months, in order to facilitate the dissolution of stone residues, the sizes of which are too small to detect, and the prevention of relapse of stone formation.