Ursosan Capsules 250mg №100

Active ingredient and dosage form

capsules white, solid, opaque gelatin.
1 capsule contains 250 mg of ursodeoxycholic acid;
Excipients:corn starch; Magnesium stearate; colloidal silicon dioxide, titanium dioxide, gelatin;
10, 50 or 100 capsules per pack.

Mechanism of action

Hepatoprotector. Ursosan also has choleretic, cholelitholytic, hypolipidemic, hypocholesterolemic and some immunomodulatory effects.
Possessing high polar properties, ursodeoxycholic acid (UDCA) 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, UDCA forms double molecules capable of being incorporated into the cell membranes of hepatocytes, cholangiocytes, gastrointestinal epithelial cells, stabilizing them and making them immune to the action of cytotoxic micelles.
By reducing the concentration of bile acids that are toxic to hepatocytes and stimulating choleresses rich in bicarbonates, ursodeoxycholic acid effectively contributes to the resolution of intrahepatic cholestasis. Reduces the saturation of bile with cholesterol due to inhibition of its absorption in the intestine,suppressing synthesis in the liver and lowering secretion to bile; increases the solubility of cholesterol in bile, forming with it liquid crystals; reduces lithogenic bile index. The result is the dissolution of cholesterol gallstones and the prevention of the formation of new stones.
The immunomodulatory effect is due to the inhibition of the expression of HLA-1 antigens on hepatocyte and HLA-2 membranes on cholangiocytes, normalization of lymphocyte natural killer activity, etc. reduces the risk of varicose veins of the esophagus. Ursodeoxycholic acid slows down the processes of premature aging and cell death (hepatocytes, cholangiocytes).

Indications and usage

- uncomplicated cholelithiasis (ICD): biliary sludge; the dissolution of cholesterol gallstones in the gallbladder, with the impossibility of their removal by surgical or endoscopic methods; prevention of recurrence of stone formation after cholecystectomy;
- chronic active hepatitis;
- acute hepatitis;
- toxic (including medicinal) liver damage;
- alcoholic liver disease;
- non-alcoholic steatohepatitis;
- primary biliary cirrhosis;
- primary sclerosing cholangitis;
- cystic fibrosis (cystic fibrosis) of the liver;
- atresia of the intrahepatic biliary tract (including congenital atresia of the bile duct);
- biliary dyskinesia;
- biliary reflux gastritis and reflux esophagitis;
- biliary dyspeptic syndrome (with cholecystopathy and biliary dyskinesia);
- prevention of liver damage when using hormonal contraceptives and cytostatics.

Dosage and administration

Capsules Ursosan take orally, drinking plenty of water.
At diffuse diseases of the liver, gallstone disease (cholesterol gallstones and biliary sludge) the drug is prescribed continuously for a long time (from several months to several years) at a daily dose of 10 mg / kg of body weight to 12-15 mg / kg (2-5 caps.).
At diffuse liver diseases The daily dose of Ursosan is divided into 2-3 doses, capsules are taken with food.
At gallstone disease the entire daily dose is taken once at night. The duration of the drug for dissolving stones - until complete dissolution, and then another 3 months for the prevention of recurrence of stone formation.
At biliary reflux gastritis and reflux esophagitis the drug is prescribed in 250 mg (1 caps.) per day, before bedtime. The course of treatment - from 10-14 days to 6 months, if necessary - up to 2 years.
After cholecystectomy, for the prevention of re-cholelithiasis The recommended dose is 250 mg 2 times / day for several months.
At toxic, medicinal lesions of the liver, alcoholic liver disease and biliary tract atresia the daily dose is established at the rate of 10-15 mg / kg / in 2-3 doses.The duration of therapy is 6-12 months or more.
At primary biliary cirrhosis the drug is prescribed at the rate of 10-15 mg / kg / day (if necessary - up to 20 mg / kg) in 2-3 doses. The duration of therapy ranges from 6 months to several years.
At primary sclerosing cholangitis - 12-15 mg / kg / day (up to 20 mg / kg) in 2-3 doses. The duration of therapy ranges from 6 months to several years.
At non-alcoholic steatohepatitis - 13-15 mg / kg / day in 2-3 doses. The duration of therapy ranges from 6 months to several years.
At cystic fibrosis the dose is set at the rate of 20-30 mg / kg / day in 2-3 doses. The duration of therapy ranges from 6 months to several years. Children over the age of 2 years set the dose of the drug individually at the rate of 10-20 mg / kg / day.

Adverse reactions

Gastrointestinal: nausea, vomiting, diarrhea (can be dose-dependent), constipation, transient (transient) increased activity of hepatic transaminases; rarely, calcification of gallstones.
Other: back pain, allergic reactions, exacerbation of previously existing psoriasis, alopecia.

Contraindications

- X-ray positive (high calcium) gallstones;
- not functioning gallbladder;
- Gastrointestinal fistula;
- acute cholecystitis;
- acute cholangitis;
- liver cirrhosis in the stage of decompensation;
- liver failure;
- renal failure;
- obturation of the biliary tract;
- acute infectious diseases of the gallbladder and bile ducts;
- empyema of the gallbladder;
- hypersensitivity to the drug.
WITH caution Ursosan capsules are used in children aged 2 to 4 years, because It may be difficult to swallow capsules, although ursodeoxycholic acid has no age limit to use.

Pregnancy and breastfeeding

AT experimental studies No mutagenic and carcinogenic effect of ursodeoxycholic acid was detected in animals. The use of ursodeoxycholic acid during pregnancy is possible only when the expected benefit to the mother outweighs the potential risk to the fetus (there are no adequate, strictly controlled studies of the use of ursodeoxycholic acid in pregnant women).
If necessary, the use of ursodeoxycholic acid during lactation should decide on the termination of breastfeeding. Data on the allocation of ursodeoxycholic acid in breast milk are currently not available.

When applied Ursosan In order to dissolve gallstones, the following conditions must be met: the stones must be cholesterol (X-ray negative), their size must not exceed 15-20 mm, the gallbladder must remain functional and must be filled with no more than half of the stones, and the patency of the cystic and common bile duct must be saved.
With prolonged (more than 1 month) administration of the drug every 4 weeks in the first 3 months of treatment, then every 3 months a biochemical blood 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 the use of Ursosan for at least 3 months in order to facilitate the dissolution of the remains of stones, the dimensions of which are too small to be detected and to prevent the recurrence of stone formation.

Drug Interactions

When used together, antacids containing aluminum and ion exchange resins (Kolestiramine) reduce the absorption of ursodeoxycholic acid. With simultaneous use, lipid-lowering drugs (especially clofibrate), estrogens, neomycin or progestins increase the saturation of bile with cholesterol and can reduce the ability of ursodeoxycholic acid to dissolve cholesterol biliary calculi.

Storage conditions

List B. Store in a dry, protected from light and out of reach of children, at a temperature of 15 - 25 ° C.
Shelf life - 4 years.