Ursosan, capsules 250 mg 10 pcs

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

With high polar properties, ursodeoxycholic acid forms non-toxic mixed micelles with apolar (toxic) bile acids, which reduces the ability of gastric refluxate 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, and GIT epitheliocytes, stabilizing them and making them immune to the action of cytotoxic micelles.

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

The immunomodulatory action is caused by inhibition of expression of HLA-1 antigens on membranes of hepatocytes and HLA-2 on cholangiocytes, normalization of natural killer activity of lymphocytes and others. Significantly delays the progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis and alcoholic steatohepatitis; reduces the risk of esophageal varices. Ursodeoxycholic acid slows premature aging and cell death (hepatocytes, cholangiocytes).

Pharmacokinetics

Absorption and distribution

Ursodeoxycholic acid is absorbed from the small intestine by passive diffusion (about 90%), and in the ileum by active transport. In this case after 30, 60 and 90 minutes after oral administration of the drug in a dose of 50 mg the concentration of ursodeoxycholic acid is 3.8 mmol/l, 5.5 mmol/l and 3.7 mmol/l, respectively. Cmax is reached after 1-3 h.

The binding to plasma proteins is high – up to 96-99%. It penetrates through the placental barrier. When taking Ursosan systematically ursodeoxycholic acid becomes the main bile acid in blood serum and is about 48% of the total amount of bile acids in blood. The therapeutic effect of the drug depends on the concentration of ursodeoxycholic acid in bile.

Metabolism and excretion

Metabolized in the liver (clearance during primary 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 with bile. A small amount of unabsorbed ursodeoxycholic acid enters the colon, where it undergoes cleavage by bacteria (7-dehydroxylation); the resulting lithocholic acid is partially absorbed from the colon, but sulfated in the liver and rapidly excreted as sulfolithocholylglycine or sulfolithocholyltaurine conjugate.

Indications

Active ingredient

Composition

Active substances:

Ursodeoxycholic acid – 250 mg.

Auxiliary substances:

corn starch – 49 mg;

corn starch pregelatinized – 24 mg;

Colloidal silica – 5 mg;

Magnesium stearate – 3.65 mg.

Capsule shell:

Gelatin – 98 mg;

Titanium dioxide – 2 mg.

How to take, the dosage

Ingestion with a small amount of water.

For 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 are completely dissolved. In case of cholelithiasis the daily dose is taken once at night.

In order to prevent recurrent calculi formation, it is recommended to use the drug for several months after their dissolution.

After cholecystectomy to prevent recurrent cholelithiasis – 250 mg 2 times a day for several months.

In chronic hepatitis of different genesis (toxic, medicinal), chronic viral hepatitis, nonalcoholic fatty liver disease, including nonalcoholic steatohepatitis, alcoholic liver disease, average daily dose – 10-15 mg/kg in 2-3 times. Duration of therapy is 6-12 months or more.

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

In biliary dyskinesia of hypokinetic type the average daily dose is 10 mg/kg in 2 intakes during 2 weeks to 2 months. It is recommended to repeat the treatment course if necessary.

In 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.

Interaction

Antacids containing aluminum and ion exchange resins (colestyramine) reduce absorption. Hypolipidemic drugs (especially clofibrate), estrogens, neomycin or progestins increase bile cholesterol saturation and may decrease the ability to dissolve cholesterol bile concretions.

Special Instructions

When taking the drug to dissolve gallstones, the following conditions must be observed: the stones must be cholesterol (X-ray non-negative), their size must not exceed 15-20 mm, the gallbladder must remain functioning and be filled by no more than half, patency of the gallbladder and common bile duct must be preserved.

When taking the drug for a long time (more than 1 month) every 4 weeks during the first 3 months of treatment, and every 3 months thereafter, biochemical blood tests should be carried out to determine the activity of liver transaminases. Control of treatment efficacy should be carried out every 6 months by ultrasonic examination of biliary tract.

After complete dissolution of the stones, it is recommended to continue treatment for at least 3 months, in order to facilitate dissolution of the remaining stones too small to be detected and to prevent recurrence of stone formation.

Contraindications

Side effects

Diarrhea (may be dose-dependent).

Rarely – calcification of gallstones, transient (transient) increase in liver transaminase activity, nausea, vomiting, abdominal pain, allergic reactions.

Overdose

Pregnancy use

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

There are currently no data on excretion of ursodeoxycholic acid with breast milk.

If it is necessary to use ursodeoxycholic acid during lactation, discontinuation of breastfeeding should be considered.

Similarities