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Active ingredients
Ursodeoxycholic acid
Release form
Capsules
Composition
Active ingredient: Ursodeoxycholic acid (Ursodeoxycholic acid) Active ingredient concentration (mg): 250 mg
Pharmacological effect
Hepatoprotector. It also has a choleretic, cholelitholytic, hypolipidemic, hypocholesterinemic and some kind of immunomodulatory effect. Having high polar properties, ursodeoxycholic acid forms non-toxic mixed micelles with apolar (toxic) bile acids, which reduces the ability of gastric refluctate to be treated with full-bodied, non-toxic, non-toxic micelles. . In addition, ursodeoxycholic acid 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. resolution of intrahepatic cholestasis. Reduces the saturation of bile with cholesterol due to inhibition of its absorption in the intestine, suppression of synthesis in the liver and a decrease in 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 calculi. The immunomodulatory effect is due to inhibition of expression of HLA-1 antigens on hepatocyte and HLA-2 membranes on cholangiocytes, normalization of the natural killer cell activity of lymphocytes and others. and alcoholic steatohepatitis; reduces the risk of varicose veins of the esophagus. Ursodeoxycholic acid slows down the processes of premature aging and cell death (hepatocytes, cholangiocytes).
Pharmacokinetics
Absorption and distribution of Ursodeoxycholic acid is absorbed from the small intestine due to passive diffusion (about 90%), and in the ileum through active transport.At the same time, the concentration of ursodeoxycholic acid when taking the drug orally at a dose of 50 mg at 30, 60, 90 min is 3.8 mmol / l, 5.5 mmol / l and 3.7 mmol / l, respectively. Cmax is reached in 1-3 hours. The binding to plasma proteins is high - up to 96-99%. It penetrates the placental barrier. When systematically taking Ursosan, ursodeoxycholic acid becomes the main bile acid in the blood serum and makes up 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 bile. Metabolism and elimination Metabolized in the liver (clearance during the initial 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. An insignificant amount of non-absorbed ursodeoxycholic acid enters the colon, where it is broken down by bacteria (7-dehydroxylation); The formed lithocholic acid is partially absorbed from the colon, but is sulfated in the liver and rapidly excreted in the form of a sulfolithocholyl glycine or sulfolithocholyl taurin conjugate.
Indications
Uncomplicated gallstone disease: 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 using hormonal contraceptives and cytostatics.
Contraindications
X-positive (high calcium) gallstones; not functioning gallbladder; 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 gallbladder; hypersensitivity to the drug.
Precautionary measures
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.
Use during pregnancy and lactation
The use of ursodeoxycholic acid during pregnancy is possible only when the expected benefit to the mother outweighs the potential risk to the fetus (adequate, well-controlled studies of the use of ursodeoxycholic acid in pregnant women have not been carried out). There is no data on the release of ursodeoxycholic acid in breast milk. If necessary, the use of ursodeoxycholic acid during lactation should decide on the termination of breastfeeding.
Dosage and administration
Ursosan is taken orally 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 JCB, the entire daily dose of the drug is taken once at night. For the prevention of re-formation of stones, it is recommended to use the drug for several months after the stones dissolve.
Side effects
Diarrhea, calcification of gallstones, transient (transient) increase in the activity of “liver” transaminases, nausea, vomiting, abdominal pain, allergic reactions.
Overdose
Cases of overdose with ursodeoxycholic acid are not known.
Interaction with other drugs
When used together, antacids containing aluminum and ion exchange resins (Kolestiramine) reduce the absorption of UDCA. When used simultaneously, lipid-lowering drugs (especially clofibrate), estrogens, neomycin, or progestins increase the saturation of bile with cholesterol and can reduce the ability of UDCA to dissolve cholesterol and increase bile cholesterol saturation and can reduce the ability of the UDCA to dissolve the cholesterin-containing cholesterol, and can reduce the amount of cholesterol that can be used to dissolve the cholesterol-absorbent substances.
special instructions
When using the drug 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; the patency of the cystic and common bile duct must be maintained. After the stones have completely dissolved, it is recommended to continue using Ursosan for at least 3 months in order to facilitate the dissolution of the residues stones whose dimensions are too small to detect them and to prevent recurrence of stone formation. In experimental animal studies, no mutagenic and carcinogenic effect was found rsodeoksiholevoy acid.