Ursofalk Capsules 250mg №100

Mechanism of action

Hepatoprotective, choleretic, immunomodulatory.
Cholelitolitichesky and antilitogenny, antifibrotic, hypocholesterolemic. It has a direct cytoprotective effect on the membrane of hepatocytes and cholangiocytes (membrane stabilizing effect). As a result of the action of the drug on the gastrointestinal circulation of bile acids, the content of hydrophobic (potentially toxic) acids decreases. By reducing the absorption of cholesterol in the intestine and other biochemical effects has a hypocholesterolemic effect. Suppresses cell death caused by toxic bile acids. It inhibits the growth of colorectal cancer cells (antitumor effect on colon cancer).
Possessing high polar properties, UDCA forms non-toxic mixed micelles with apolar (toxic) bile acids, which reduces the ability of gastric reflux to damage cell membranes during biliary reflux gastritis and reflux esophagitis. In addition, UDCA forms double molecules that can be incorporated into cell membranes, stabilize them, and make them immune to the action of cytotoxic micelles. 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 antigens on the membranes of hepatocytes and cholangiocytes, normalization of the natural killer activity of lymphocytes, etc. Reliably retards the progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis and alcoholic hepatitis, relies on the risk of developing the condition.

For successful dissolution of gallstones, it is necessary that the stones be purely cholesterol, their size does not exceed 15–20 mm, and the gallbladder (filled with stones no more than half) and the bile-excreting paths fully preserve their function.

Indications and usage

- primary biliary cirrhosis;
- primary sclerosing cholangitis;
- chronic active hepatitis;
- cystic fibrosis;
- Atresia of the intrahepatic biliary tract;
- cholestasis with parenteral nutrition;
- alcoholic liver damage;
- acute hepatitis;
- prevention of liver damage when using hormonal contraceptives, treatment with cytostatics (during transplantation);
- cholesterol gallstones in the gall bladder (in the absence of the possibility of their removal by surgicalor endoscopic methods);
- biliary reflux gastritis and reflux esophagitis;
- biliary dyskinesia;
- Prevention of colon cancer in patients with a high risk of its development (for example, ulcerative colitis).

Contraindications

 
- hypersensitivity to the drug;
- X-ray (high calcium) gallstones;
- non-functioning gallbladder,
- acute inflammatory diseases of the gallbladder, bile ducts and intestines,
- cirrhosis in the stage of decompensation,
- pronounced dysfunction of the kidneys, liver, pancreas,
- pregnancy, breastfeeding.

Dosage and administration

Inside, at bedtime (capsules - without chewing and washing down with a small amount of liquid), in the treatment of gallstone disease - 1 time per day before bedtime; for liver diseases - 2-3 times a day.
Suspension Recommended for use in children and in patients with difficulty swallowing.
For treatment acute and chronic liver diseases, to dissolve gallstones Ursofalk is used in a dose of 10 mg / kg / day (2-5 capsules or 10-25 ml of suspension, respectively) to 12-15 mg / kg continuously for a long time. In the treatment of chronic liver diseases, the duration of treatment can range from several months to 2 years. The duration of the process of dissolution of gallstones when using Ursofalk is from 6 months to 2 years.If after 12 months from the beginning of the application, no decrease in gallstones is observed, then it is not advisable to continue the treatment.
For treatment biliary reflux gastritis and reflux esophagitis appoint 250 mg at bedtime, capsule. Duration of administration is usually 10-14 days.
Primary biliary cirrhosis: 10-15 mg / kg / day (if necessary, up to 20 mg / kg) for 6-24 months (up to several years).
Primary sclerosing cholangitis: 12-15 mg / kg / day (up to 20 mg / kg) for 6-24 months (up to several years).
Cystic fibrosis (cystic fibrosis): up to 20-30 mg / kg / day for 6-24 months or more.
Toxic and alcoholic liver damage: 10-15 mg / kg / day for 6-12 months or more.

Adverse reactions

In some cases: diarrhea, calcification of gallstones.
In the treatment of primary biliary cirrhosis, transient decompensation of cirrhosis of the liver may occur, which disappears after discontinuation of the drug.

Pregnancy and breastfeeding

Before starting treatment with Ursofalk, pregnancy should be excluded.
Women of childbearing age during the period of use of the drug is recommended to use non-hormonal contraception or oral hormonal contraceptives with a low content of estrogen.
Data on the allocation of ursodeoxycholic acid in breast milk are currently not available. If necessary, use Ursofalk during lactation should decide on the termination of breastfeeding.

Special notes

When prescribing Ursofalk to dissolve gallstones in order to monitor the effectiveness of treatment, it is recommended to conduct x-ray and ultrasound of the biliary tract every 6 months.
In cholestatic liver diseases, the activity of transaminases, alkaline phosphatase and gamma-glutamyltranspeptidase in the blood serum should be periodically determined.
There is evidence of the use of Ursofalk with cholestasis during pregnancy.
For successful litholysis using Ursofalk, the following conditions must be met: the stones must be purely cholesterol, i.e. do not give a shadow on the radiograph; the size of the stones should not exceed 15-20 mm; the gallbladder must fully preserve its function; the gallbladder should be filled with stones no more than half; patency of the cystic duct should be maintained; the common bile duct should be free from stones.
When prescribing Ursofalk to dissolve cholesterol stones, one should not simultaneously use drugs that increase cholesterol in bile (for example, estrogens, clofibrate).
To prevent the recurrence of cholelithiasis, treatment should continue for several months after the gallstones dissolve.
The raw materials used in the manufacture of the drug, there is a certificate confirming the absence of the virus Jakob-Cocurfeldt.

Drug Interactions

Kolestiramine or antacids containing aluminum hydroxide bind ursodeoxycholic acid in the intestine, thereby preventing its absorption and reduce the effectiveness of Ursofalk (this combination is not appropriate).
With simultaneous use with the drug Ursofalk (in patients who have undergone organ transplantation) may increase the absorption of cyclosporine.

Storage conditions

The drug should be stored in a dry, dark place at room temperature.