Ursosan, capsules 250mg, 100pcs

Composition

Active ingredient:  

ursodeoxycholic acid – 250 mg.

Auxiliary substances:  

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

Pharmacological action

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

Having 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, and gastrointestinal epithelial cells, stabilize them and make them immune to the action of cytotoxic micelles.

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

The immunomodulatory effect is due to inhibition of the expression of HLA-1 antigens on hepatocyte membranes and HLA-2 on cholangiocytes, normalization of the natural killer activity of lymphocytes, etc. Significantly delays the progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis and alcoholic steatohepatitis; reduces the risk of esophageal varicose veins. 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 by passive diffusion (about 90%), and in the ileum by active transport. At the same time, the concentration of ursodeoxycholic acid when taking the drug orally 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.

Binding to plasma proteins is high – up to 96-99%. Penetrates the placental barrier. When Ursosan is taken systematically, ursodeoxycholic acid becomes the main bile acid in the blood serum and accounts for 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 the bile.

Metabolism and elimination

It is metabolized in the liver (clearance during primary passage through the liver) to 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 unabsorbed ursodeoxycholic acid enters the colon, where it is broken down by bacteria (7-dehydroxylation); the resulting litocholic acid is partially absorbed from the colon, but is sulfated in the liver and quickly excreted as a sulfolitocholylglycine or sulfolitocholyltaurine conjugate.

Indications

-Uncomplicated cholelithiasis (GI): biliary sludge; dissolution of cholesterol gallstones with a functioning gallbladder; prevention of relapses of stone formation after cholecystectomy;- Chronic hepatitis of various origins (toxic, medicinal, etc. ); – Cholestatic liver diseases of various origins, including primary biliary cirrhosis, primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis);- Non-alcoholic fatty liver disease, including non-alcoholic steatohepatitis;- Alcoholic liver disease;- Chronic viral hepatitis;- Biliary dyskinesia;- Biliary reflux-gastritis and reflux esophagitis.

Use during pregnancy and lactation

The use of ursodeoxycholic acid during pregnancy is possible only if the expected benefit to the mother exceeds 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 excretion of ursodeoxycholic acid in breast milk are currently unavailable. If it is necessary to use ursodeoxycholic acid during lactation, the question of stopping breastfeeding should be decided.

Contraindications

• Roentgenologically (high in calcium) gallstones;
• not functioning gall bladder
• biliary-gastrointestinal fistula;
• acute cholecystitis,
• acute cholangitis;
• cirrhosis of the liver in the stage of decompensation;
• liver failure;
• renal failure;
• obstruction of the biliary tract;
• acute infectious diseases of the gallbladder and bile ducts;
• empyema of the gall bladder;
• hypersensitivity to the components of the drug.

Use Ursosan with caution: in children aged 2 to 4 years, as it may be difficult to swallow capsules, although ursodeoxycholic acid has no age restrictions in use.

Side effects

Diarrhea (may be dose-dependent).

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

Interaction

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

How to take, course of use and dosage

Inside, with a small amount of 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 or more until the stones completely dissolve. With gallstone disease, the entire daily dose of the drug is taken once at night.

To prevent the 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 recurrent cholelithiasis — 250 mg 2 times a day for several months.

For chronic hepatitis of various origins (toxic, medicinal), 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.

For cholestatic liver diseases 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.

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

For 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.

Overdose

Cases of overdose with ursodeoxycholic acid are not known.

Special instructions

When taking the drug for the purpose of dissolving 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 stones no more than half, the patency of the cystic and common bile duct should be preserved.

If the drug is taken for a long time (more than 1 month) every 4 weeks in the first 3 months of treatment, and then every 3 months, a biochemical blood test should be performed to determine the activity of hepatic transaminases. Monitoring of the effectiveness of treatment should be carried out every 6 months according to ultrasound of the biliary tract.

After the stones are completely dissolved, it is recommended to continue using the drug for at least 3 months, in order to promote the dissolution of stone residues, the size of which is too small for their detection, and prevent the recurrence of stone formation.

Form of production

Capsules

Storage conditions

Store in a dry place, protected from light, at a temperature of 15-25 °C. Keep out of reach of children.

Shelf

life is 4 years.

Active ingredient

Ursodeoxycholic acid

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Purpose

For adults as directed by your doctor

Indications

Cholelithiasis, Cirrhosis of the liver