Ursodeoxycholic acid (Ursosan) 250 mg – [50 capsules]

Hepatoprotective drug, also has a choleretic, cholitholytic, hypolipidemic, hypocholesterolemic and some immunomodulatory effects.

Having high polar properties, ursodeoxycholic acid (UDCA) is embedded in the membrane of hepatocyte, cholangiocyte and gastrointestinal epithelial cell, stabilizes its structure and protects the cell from the damaging effects of toxic bile acids salts, thus reducing their cytotoxic effect. It 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. By reducing concentrations and stimulating bicarbonate-rich choleresis, UDCA is effective in resolving intrahepatic cholestasis. In cholestasis it activates Ca2+-dependent alpha-protease and stimulates exocytosis, decreases concentration of toxic bile acids (chenodeoxycholic acid, lithocholic acid, deoxycholic acid, etc.), which concentrations are elevated in patients with chronic liver disease.

Competitively reduces absorption of lipophilic bile acids in intestine, increases their “fractional” turnover in enterohepatic circulation, induces choleresis, stimulates bile passage and excretion of toxic bile acids through intestine. It decreases bile saturation with cholesterol due to inhibiting its absorption in intestine, inhibiting its synthesis in liver and decreasing its secretion into bile; it increases cholesterol solubility in bile, forming liquid crystals with it; it decreases bile lithogenic index, increases concentration of bile acids in it, causes intensification of gastric and pancreatic secretion, increases lipase activity, produces hypoglycemic effect. Causes partial or complete dissolution of cholesterol gallstones, decreases bile cholesterol saturation, which promotes its mobilization from gallstones. The result is the dissolution of cholesterol gallstones and the prevention of the formation of new concrements. Immunomodulatory action is caused by inhibition of expression of histocompatibility antigens – HLA-1 – on membranes of hepatocytes and HLA-2 – on cholangiocytes, normalization of natural killer activity of lymphocytes, formation of interleukin-2, decrease of eosinophils amount, suppression of immunocompetent immunoglobulins (Ig), especially IgM. Delays the progression of fibrosis. Regulates the processes of apoptosis of hepatocytes, cholangiocytes and epitheliocytes of the gastrointestinal tract.

– Uncomplicated cholelithiasis (GBS): biliary sludge, dissolution of cholesterol gallstones with a functioning gallbladder, the prevention of recurrence of stone formation after cholecystectomy.

– Chronic hepatitis of different genesis (toxic, medicinal, etc.)

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

– Nonalcoholic fatty liver disease, including nonalcoholic steatohepatitis

– Alcoholic liver disease

– Chronic viral hepatitis

– Biliary dyskinesia

– Biliary reflux gastritis and reflux esophagitis.

Hypersensitivity, X-ray-positive (high in calcium) gallstones, non-functioning gallbladder, marked renal, hepatic, pancreatic disorders, decompensated liver cirrhosis, acute biliary tract infection and inflammatory diseases.

Ursodeoxycholic acid has no age restrictions for use, but it is not recommended for children under 3 years of age to use the drug in this dosage form.

Pregnancy and lactation:

The use of UDCA in pregnancy is possible only when the expected benefit to the mother exceeds the potential risk to the fetus. There are currently no data on excretion of ursodeoxycholic acid with breast milk. If it is necessary to use UDCA during lactation, discontinuation of breastfeeding should be considered.

 

• Inside, 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. For cholelithiasis the entire daily dose is taken once at night.
• To prevent recurrent stone formation, it is recommended that the drug be used for several months after the dissolution of stones.
• After cholecystectomy to prevent recurrent cholelithiasis – 250 mg 2 times a day for several months.
• In chronic hepatitis of different genesis (toxic, medicinal, etc.), chronic viral hepatitis, nonalcoholic fatty liver disease, including nonalcoholic steatohepatitis, alcoholic liver disease average daily dose is 10-15 mg/kg 2-3 times. The duration of therapy is 6-12 months or more.
• In cholestatic hepatic diseases of different genesis, including: primary biliary cirrhosis, primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis) an average daily dose is 12-15 mg/kg; if necessary, daily dose can be increased up to 20-30 mg/kg in 2-3 doses. Duration of therapy ranges 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. If necessary, it is recommended to repeat the treatment course.
• In biliary reflux gastritis and reflux esophagitis – 250 mg daily, before sleep. The course of treatment – from 10-14 days to 6 months, if necessary – up to 2 years.
• Calculation of daily number of capsules depending on the body weight and recommended dose per 1 kg of body weight (mg/kg/day)
• body weight 10 mg/kg/day 12 mg/kg/day 15 mg/kg/day 20 mg/kg/day 30 mg/kg/day
• 19-25 kg 1 capful 1 capful 2 capful 3 capful
• 26-30 kg 1 capful 1 capful 2 capful 2 capful 4 capful
• 31-35 kg 1 capful 2 capsules 2 capsules 3 capsules 4 capsules
• 36-40 kg 2 capts 2 capts 2 capts 3 capts 5 capts
• 41-45 kg 2 capts 2 capts 3 capts 4 capts 5 capts
• 45-50 kg 2 capts 2 capts 3 capts 4 capts 6 capts
• 51-55 kg 2 capts 3 capts 3 capts 4 capts 7 capts
• 56-60 kg 2 capts 3 capts 4 capts 5 capts 7 capts
• 61-65 kg 3 captions 3 captions 4 captions 5 captions 8 captions
• 66-70 kg 3 captions 3 captions 4 captions 6 captions 8 captions
• 71-75 kg 3 captions 4 captions 5 captions 6 captions 9 captions
• 76-80 kg 3 captions 4 captions 5 captions 6 captions 10 captions
• 81-85 kg 3 captions 4 captions 5 captions 7 captions 10 captions
• 86-90 kg 4 captions 4 captions 5 captions 7 captions 11 captions
• 91-95 kg 4 captions 5 captions 6 captions 8 captions 11 captions
• 96-100 kg 4 captions 5 captions 6 captions 8 captions 12 captions
• 101-105 kgs 4 captions 5 captions 6 captions 8 captions 13 captions
• 105-110 kgs 4 captives 5 captives 7 captives 9 captives 13 captives