Ursodez, capsules 250 mg 100 pcs

Pharmacotherapeutic drug group:

Hepatoprotective agent

ATX code: [A05AA02]

Pharmacological properties

Pharmacodynamics

Hepatoprotective drug, has a choleretic effect. It reduces the synthesis of cholesterol in the liver, its absorption in the intestine and its concentration in the bile, increases the solubility of cholesterol in the biliary system, stimulates the formation and excretion of bile.

Lithogenicity of bile decreases, increases the content of bile acids in it; causes intensification of gastric and pancreatic secretion, increases lipase activity, has hypoglycemic effect. Causes partial or complete dissolution of cholesterol stones in enteral administration, reduces the saturation of bile with cholesterol, which promotes the mobilization of cholesterol from gallstones.

It has immunomodulatory effects, affects immunological reactions in the liver: decreases the expression of some antigens on the membrane of hepatocytes, affects the number of T-lymphocytes, interleukin-2 formation, decreases 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 administration in a single dose (500 mg), maximum serum concentration (Cmax) after 30, 60, 90 min is 3.8, 5.5, 3.7 mmol/l, respectively. The binding to plasma proteins is high – up to 96-99%.

It penetrates through the placental barrier. With systematic administration of ursodeoxycholic acid becomes the main bile acid of blood serum (48% of total bile acids). The therapeutic effect of the drug depends on the concentration of UDCA in bile.

It is metabolized in the liver (clearance by “primary passage” through the liver) into 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 undergoes cleavage by bacteria (7-dehydroxylation); the resulting lithocholic acid is partially absorbed from the colon, but is sulfated in the liver and rapidly excreted as sulfolithocholylglycine or sulfolithocholyltaurine conjugate.

Indications

Active ingredient

Composition

1 capsule contains:

the active ingredient:

ursodeoxycholic acid – 250 mg,

excipients:

Pregelatinized starch (starch 1500) – 73.0 mg,

colloidal silica (aerosil) – 5.0 mg,

magnesium stearate – 2.0 mg,

capsule shell:

titanium dioxide,

gelatin

How to take, the dosage

Intravenously.

Dissolution of 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), with a small amount of liquid. Duration of treatment 6-12 months. Administration of the drug for several months after stone dissolution is recommended to prevent recurrent cholelithiasis.

Treatment of biliary reflux gastritis

1 capsule of Ursodez daily in the evening before going to bed with a small amount of water. The course of treatment from 10-14 days to 6 months, if necessary – up to 2 years.

The symptomatic treatment of primary biliary cirrhosis

Daily dose depends on body weight and consists of 2 to 6 capsules (about 10 to 15 mg of ursodeoxycholic acid per 1 kg of body weight) in 2-3 intakes.

In chronic hepatitis of different genesis, nonalcoholic steatohepatitis and alcoholic liver disease

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

In 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 may be increased to 20-30 mg per 1 kg of body weight in 2-3 doses. The duration of therapy ranges from 6 months to several years.

In biliary dyskinesia

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

Interaction

Colestyramine, colestipol and antacids containing aluminum hydroxide or smectite (aluminum oxide) reduce 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 can increase absorption of cyclosporine from the intestine. Therefore, in patients taking cyclosporine, the physician should check the cyclosporine concentration in blood and adjust the dose of cyclosporine if necessary.

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

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 recurrence of cholelithiasis. In cholestatic diseases of the liver serum activity of transaminases, alkaline phosphatase and GGTP should be determined periodically.

Impact on the ability to drive and operate machinery. There are no data on the effect of UDCA on the ability to drive vehicles and operate machinery.

Contraindications

Side effects

Overdose

No cases of overdose have been identified. In case of overdose symptomatic treatment is administered.

Pregnancy use

The drug is contraindicated during pregnancy and lactation.

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