Ursofalk, capsules 250 mg 50 pcs

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 the prevention of the formation of new concrements.

The immunomodulatory activity is caused by inhibition of HLA-antigens expression on membranes of hepatocytes and 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 developing esophageal varices.

For 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.

Therapeutic effectiveness of the drug depends on the concentration of UDCA in bile. On the background of the therapy there is dose-dependent increase of UDCA share in the bile acid pool up to 50-75% (with daily doses of 10-20 mg/kg). It penetrates through the placental barrier.

Indications

Active ingredient

Composition

Active ingredient:

Ursodeoxycholic acid 250 mg.

Auxiliary substances:

magnesium stearate,

corn starch,

colloidal anhydrated silicon dioxide,

How to take, the dosage

Dissolution of cholesterol gallstones

Approximately 10 mg per 1 kg body weight daily, which corresponds to:

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.

Blockage of common bile duct or vesicular duct.

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.

Similarities