Ursofalk, 250 mg/5 ml suspension 250 ml

Pharmacodynamics

With high polar properties UDCA forms non-toxic mixed micelles with apolar (toxic) bile acids, which reduces the ability of refluxate to damage cell membranes in biliary reflux gastritis and reflux esophagitis. In addition, UDCA forms double molecules capable of incorporating into cell membranes, stabilizing them and making them immune to the action of cytotoxic micelles.

Limits the saturation of bile with cholesterol by inhibiting its absorption in the intestine, suppressing its synthesis in the liver and reducing its secretion into the bile; increases the solubility of cholesterol in bile, forming liquid crystals with it; reduces the lithogenic index of bile. The result is the dissolution of cholesterol gallstones and prevention of formation of new concrements.

The immunomodulatory activity is caused by inhibition of expression of HLA-antigens on membranes of hepatocytes and cholangiocytes and normalization of natural killer activity of lymphocytes.

It significantly delays the progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis and alcoholic steatohepatitis and reduces the risk of varicose esophageal veins.

For the successful dissolution of gallstones, it is necessary that the stones are pure cholesterol stones, their size does not exceed 15-20 mm, and the gallbladder (filled with stones no more than half) and the biliary tract fully retain their function.

Pharmacokinetics

Absorbed in the jejunum by passive diffusion, in the ileum by active transport. When administered orally in a single dose of 500 mg, serum concentration after 30, 60 and 90 minutes is 3.8, 5.5 and 3.7 μmol/L, respectively.

When taken systematically ursodeoxycholic acid (UDCA) becomes the main bile acid of blood serum (48% of total bile acids). It is included in the enterohepatic circulation system. The therapeutic effectiveness of the drug depends on the concentration of UDCA in bile.

With the background of therapy there is dose-dependent increase of UDCA share in the bile acid pool up to 50-75% (at daily doses of 10-20 mg/kg). It penetrates the placental barrier.

Indications

Active ingredient

Composition

Active substance:

Ursodeoxycholic acid 250 mg.

Auxiliary substances:

benzoic acid,

avicel RC 591,

sodium chloride,

sodium citrate,

citric acid,

glycerin,

propylene glycol,

xylitol,

sodium cyclamate,

Givaudan lemon flavoring 87017,

purified water.

How to take, the dosage

For dissolution of cholesterol gallstones 10 mg/kg body weight 1 time/day is prescribed.

The duration of treatment is 6-12 months.

For prevention of recurrent cholelithiasis it is recommended to take the drug for several months after dissolution of stones.

To treat biliary reflux gastritis we prescribe 1 scoop of Ursofalk once a day. The course of treatment is from 10-14 days to 6 months, if necessary – up to 2 years.

For symptomatic treatment of primary biliary cirrhosis daily dose depends on body weight and is from 2 to 6 scoops (about 10-15 mg/kg of body weight).

Interaction

Cholestyramine, colestipol and antacids containing aluminum hydroxide bind ursodeoxycholic acid in the intestine, prevent its absorption and weaken its effectiveness (simultaneous use is not advisable).

Contraindications

Acute inflammatory diseases of the gallbladder and bile ducts.

Bile duct or vesicular duct obstruction.

Side effects

Diarrhea, nausea, pain in the epigastric region and the right subcostal area; calcification of gallstones; increased activity of liver transaminases (AST, ALT).

Allergic reactions.

In treatment of primary biliary cirrhosis transient decompensation of cirrhosis of the liver may be observed, which disappears after discontinuation of the drug.

Overdose

There are no data on overdose.

Pregnancy use

There are published data on the use of the drug during pregnancy.

The use of the drug should currently be limited to the second and third trimesters of pregnancy.

There are no data on penetration into breast milk.

Similarities