Ursodez capsules 500mg №30

Ursodez®

ursodeoxycholic acid

Dosage form

capsules

Hepatoprotective agent

Pharmacology

Pharmacodynamics

Hepatoprotective agent, has a choleretic effect. Reduces synthesis

cholesterol in the liver, its absorption in the intestine and concentration in the bile, increases the solubility of cholesterol in the biliary system, stimulates the formation and secretion of bile. Reduces the lithogenicity of bile, increases the content of bile acids; causes an increase in gastric and pancreatic secretion, enhances the activity of lipase, has a hypoglycemic effect. Causes partial or complete dissolution of cholesterol stones

with enteral administration, reduces the saturation of bile with cholesterol, which helps mobilize cholesterol from gallstones. It has an immunomodulatory effect, affects the immunological reactions in the liver: reduces the expression of certain antigens on the membrane of hepatocytes,

affects the number of T-lymphocytes, the formation of interleukin-2, reduces the number of eosinophils.

Pharmacokinetics

Ursodeoxycholic acid (UDCA) is absorbed in the small intestine due to passive

diffusion (about 90%), and in the ileum through active transport. After ingestion in a single dose (500 mg), the maximum concentration in serum (Cmax) after 30, 60, 90 min is 3.8, 5.5, 3.7 mmol / l, respectively. Communication with plasma proteins - high - up to 96-99%.

It penetrates the placental barrier. When taken systematically, ursodeoxycholic acid becomes the main bile acid of blood serum (48% of the total bile acid content). The therapeutic effect of the drug depends on the concentration of UDCA in the bile. Metabolized in the liver.

(clearance in the "primary passage" through the liver) in Taurine and Glycine

conjugates. The resulting conjugates are secreted into the bile. About 50-70% of the total dose is excreted through the intestines. Insignificant amount of non-absorbed urso

deoxycholic 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 and usage

Dissolution of cholesterol gallstones, biliary reflux

- gastritis, primary biliary cirrhosis in the absence of signs of decompensation (symptomatic treatment). Chronic hepatitis of various genesis, primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis), non-alcoholic steatohepatitis, alcoholic liver disease, biliary dyskinesia.

Contraindications

- X-ray positive (high calcium) gallstones;

-Difunctioning gallbladder;

- Acute inflammatory diseases of the gallbladder, bile ducts and intestines;

-Cirrhosis in the stage of decompensation;

Severely impaired function of the liver, kidneys, pancreas;

- Increased sensitivity to the components of the drug;

- Adults and children weighing up to 34 kg.

Inside

Dissolution of cholesterol gallstones

The recommended (approximate) dose is 10 mg urs

odesoxycholic acid per 1 kg of body weight per day. The drug must be taken daily in the evening, before bedtime (capsules are not chewed), washed down with a small amount of liquid. The duration of treatment is 6-12 months. For the prevention of re-cholelithiasis, it is recommended to take the drug for several months after the stones dissolve.

Treatment of biliary reflux gastritis 1 capsule of the drug Ursodez® daily in the evening before bedtime, washing down with a small amount of water. The course of treatment from 10

-14 days to 6 months, if necessary, up to 2 years.

Symptomatic treatment of primary biliary cirrhosis

The daily dose depends on body weight and ranges from 2 to 6 capsules (approximately 10 to 15 mg of ursodeoxycholic acid per 1 kg of body weight) in 2-3 doses.

In chronic hepatitis of various origins, non-alcoholic steatohepatitis and

alcoholic liver disease

The average daily dose is from 10 to 15 mg of ursodeoxycholic acid per 1 kg of body weight in 2-3 doses. The duration of therapy is 6-12 months or more.

In primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis)

The average daily dose ranges from 12 to 15 mg of ursodeoxycholic acid per 1 kg of body weight; if necessary, the average daily dose can be increased to 20-30 mg per 1 kg of body weight in 2-3 doses. The duration of therapy is from 6 months to several years.

When biliary dyskinesia

The average daily dose is 10 mg of ursodeoxycholic acid per 1 kg of body weight in 2 doses for 2 weeks to 2 months. If necessary, the course of treatment must be repeated.

Special notes

In cholelithiasis, treatment efficacy is monitored every 6 months by performing x-ray and ultrasound of the biliary tract to prevent recurrence of cholelithiasis. In cholestatic liver diseases, the activity of transaminases, alkaline phosphatase and gamma-glutamyltranspeptidase in the blood serum should be periodically determined.

Overdosage

No cases of overdose have been identified. In case of overdose, symptomatic treatment is carried out.

Diarrhea, nausea, pain in the epigastric and right hypochondrium, calcification of gallstones, increased activity of liver transaminases, allergic reactions. In the treatment of primary biliary cirrhosis, transient decompensation of cirrhosis of the liver may occur, which disappears after discontinuation of the drug.

Drug interactions

Kolestiramin, colestipol and antacids containing aluminum hydroxide or smectite (aluminum oxide) reduce the absorption of ursodeoxycholic acid in the intestine and thus reduce its absorption and effectiveness. If the use of drugs containing at least one of these substances is still necessary, they should be taken at least 2 hours before taking Ursodez®. Ursodeoxycholic acid can enhance the absorption of cyclosporine from the intestine. Therefore, in patients taking cyclosporine, the doctor must check the concentration of cyclosporine in the blood and adjust the dose of cyclosporine if necessary. In some cases, Ursodez® may reduce the absorption of Ciprofloxacin. Lipid-lowering drugs (especially clofibrate), estrogens, neomycin, or progestins increase the saturation of bile with cholesterol and may decrease the ability to dissolve cholesterol biliary stones.

The drug is contraindicated during pregnancy and lactation.

There is no data on the effect of ursodeoxycholic acid on the ability to manage

vehicles and work with mechanisms.

Storage conditions

In a dry, dark place, at a temperature not higher than 25 ° C. Keep out of the reach of children.