Ursodez, capsules 250mg, 100pcs

Composition

1 capsule contains:

Active ingredient:  

ursodeoxycholic acid – 250 mg,

excipients:  

pregelatinized starch (starch 1500) – 73.0 mg,

colloidal silicon dioxide (aerosil) – 5.0 mg,

magnesium stearate-2.0 mg,

capsule shell:  

titanium dioxide,

gelatin

Pharmacological action

PHARMACOTHERAPEUTIC GROUP OF THE DRUG:

Hepatoprotective agent

ATX CODE: [A 05 AA 02]

PHARMACOLOGICAL PROPERTIES

Pharmacodynamics

Hepatoprotective agent, has a choleretic effect. Reduces the synthesis of cholesterol in the liver, its absorption in the intestines and concentration in bile, increases the solubility of cholesterol in the biliary system, stimulates the formation and excretion of bile.

Reduces the lithogenicity of bile, increases the content of bile acids in it; causes increased gastric and pancreatic secretion, increases the activity of lipase, has a hypoglycemic effect. Causes partial or complete dissolution of cholesterol stones with enteral application, reduces the saturation of bile with cholesterol, which contributes to the mobilization of cholesterol from gallstones.

It has an immunomodulatory effect, affects immunological reactions in the liver: reduces the expression of certain antigens on the hepatocyte membrane, affects the number of T-lymphocytes, interleukin-2 formation, reduces the number of eosinophils.

Pharmacokinetics

Ursodeoxycholic acid (UDCA) is absorbed in the small intestine by passive diffusion (about 90%), and in the ileum by active transport. After oral use in a single dose (500 mg), the maximum serum concentration (Cmax) after 30,60,90 minutes is 3.8,5.5, and 3.7 mmol/l, respectively. The relationship with plasma proteins is high – up to 96-99%.

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

It is metabolized in the liver (clearance during “primary passage” through the liver) to taurine and glycine conjugates. The resulting conjugates are secreted into the bile. About 50-70% of the total dose is excreted through the intestine. A small amount of unabsorbed ursodeoxycholic acid enters the large intestine, where it is broken down by bacteria (7-dehydroxylation); the resulting litocholic acid is partially absorbed from the colon, but is sulfated in the liver and is quickly excreted as a sulfolitocholylglycine or sulfolitocholyltaurine conjugate.

Indications

• Dissolution of cholesterol gallstones;
• primary biliary cirrhosis in the absence of signs of decompensation (symptomatic therapy);
• biliary reflux gastritis;
• chronic hepatitis of various origins;
• primary sclerosing cholangitis;
• cystic fibrosis (cystic fibrosis);
• non-alcoholic steatohepatitis;
• alcoholic liver disease;
• biliary dyskinesia.

Use during pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Contraindications

• Hypersensitivity to the drug Arcades;
• roentgenologically (high in calcium) gallstones;
• nonfunctioning gallbladder;
• acute inflammatory diseases of the gallbladder, bile ducts and intestines;
• liver cirrhosis in the stage of decompensation;
• pronounced violations of the liver, kidney, pancreas;
• pancreatitis;
• pregnancy;
• lactation;
• adults and children weighing up to 34 kg.

Side effects

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

Interaction

Colestyramine, colestipol and antacids containing aluminum hydroxide or smectite (aluminum oxide) reduce the absorption of UDCA 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.

UDCA may increase the absorption of cyclosporine from the intestine. Therefore, in patients taking cyclosporine, the doctor should check the concentration of cyclosporine in the blood and adjust the dose of cyclosporine if necessary.

In some cases, Ursodesis may reduce the absorption of ciprofloxacin. Hypolipidemic drugs (especially clofibrate), estrogens, neomycin, or progestins increase bile saturation with cholesterol and may reduce the ability to dissolve cholesterol bile stones.

How to take, course of use and dosage

Inside.

Dissolving cholesterol gallstones

The recommended (approximate) dose is 10 mg of ursodeoxycholic acid per 1 kg of body weight per day. The drug should be taken daily in the evening, before going to bed (capsules are not chewed), washed down with a small amount of liquid. The duration of treatment is 6-12 months. To prevent recurrent cholelithiasis, it is recommended to take the drug for several months after the dissolution of the stones.

Treatment of biliary reflux gastritis

1 capsule of Ursodez daily in the evening before going to bed, washed down with a small amount of water. The course of treatment is 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.

With 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.

For primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis)

The average daily dose is 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.

With 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 should be repeated.

Overdose

No cases of overdose were detected. In case of overdose, symptomatic treatment is performed.

Special instructions

In cholelithiasis, the effectiveness of treatment is monitored every 6 months by X-ray examination and ultrasound of the biliary tract in order to prevent relapses of cholelithiasis. In cholestatic liver diseases, the activity of transaminases, ALP and GGTP in the blood serum should be periodically determined.

Influence on the ability to drive motor vehicles and manage mechanisms. There are no data on the effect of UDCA on the ability to drive vehicles and work with mechanisms.

Form of production

Capsules

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

5 years

Active ingredient

Ursodeoxycholic acid

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Description

For adults as directed by your doctor

Indications

Cirrhosis of the liver, Cholelithiasis