Ursodez, capsules 250mg 120pcs

Composition

Active ingredient: Ursodeoxycholic acid-250 mgcompetitive substances:  pregelatinized starch (starch 1500) – 73.0 mg, colloidal silicon dioxide (aerosil) – 5.0 mg, magnesium stearate-2.0 mg capsule shell: body and lid: titanium dioxide-2.1118%, gelatin – up to 100%

Pharmacological action

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 when applied orally, 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, the formation of interleukin-2, 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 undergoes cleavage 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 sulfolitocholylglycime or sulfolitocholyltaurine conjugate.

Indications

Dissolution of small and medium-sized cholesterol stones with a functioning gallbladder, biliary reflux gastritis, primary biliary cirrhosis of the liver in the absence of signs of decompensation (symptomatic treatment).

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

• X-ray positive (with a high calcium content) gallstones;
• Mefumkciomiruyushchy gall bladder;
• Acute inflammatory diseases of the gallbladder, bile ducts and intestines;
• Liver cirrhosis in the stage of decompensation;
• Severe disorders of the liver, kidneys, and pancreas;
• Hypersensitivity to the components of the drug;
• Adults and children weighing up to 34 kg.
• Children under 3 years of age, for this dosage form.

With caution

Use with caution in the following conditions: cholelithiasis, cholestatic liver diseases (see the section “Special instructions”).

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 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 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, Ursodez® may reduce the absorption of ciprofloxacin. Lipid-lowering medications (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.

It usually takes 6-24 months for gallstones to dissolve. If the size of the stones does not decrease after 12 months of treatment, then the treatment should be discontinued.

The effectiveness of treatment should be evaluated every 6 months by ultrasound or radiography. During the interim survey, it is necessary to assess whether calcification of stones has occurred during the elapsed period. In case of calcification of stones, treatment should be discontinued.

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 (250 mg) 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 is from 1 to 3 capsules (500 mg) or from 2 to 6 capsules (250 mg) (approximately 10 to 15 mg of Ursodeoxycholic acid per 1 kg of body weight) in 2 to 3 doses, the first 3 months of treatment. After improving the functional parameters of the liver, the daily dose can be applied once in the evening.

The duration of treatment is unlimited. In rare cases, at the beginning of treatment, clinical symptoms may worsen (pruritus may become more frequent). In this case, the daily dose should be reduced (up to 250 mg), and then gradually increased (weekly increasing the daily dose) until the recommended dosage regimen is reached.

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)

For primary sclerosing cholangitis: 12-15 mg / ct / day (up to 20 mg/kg) of body weight per day in 2-3 doses. Duration of application-from 6 months to several years. Cystic fibrosis (cystic fibrosis): 20-30 mg / kg per day in 2-3 doses. Duration of application-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.

The dosage regimen is determined by the doctor.

Table. Calculation of the daily number of capsules depending on the patient’s body weight and the recommended dose of the drug pa 1 kg of body weight

For children over 3 years old Individually (at the rate of 10-20 mg / kg per day).

Overdose

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

Special instructions

Ursodez® should be administered under medical supervision. During the first 3 months of treatment, liver function parameters (transaminases, alkaline phosphatase, and gamma – glutamyltranspeptidase) in the blood serum should be monitored every 4 weeks, and then every 3 months.

Monitoring of these parameters allows detecting liver function disorders in the early stages. This also applies to patients in the late stages of primary biliary cirrhosis. In addition, it can quickly determine whether a patient with primary biliary cirrhosis is responding to treatment.

When used to dissolve cholesterol gallstones:

In order to assess progress in treatment and for timely detection of signs of calcification of stones, the gallbladder should be visualized (oral cholecystography) with examination of darkening in the “standing” and “lying on your back” positions (ultrasound) 6-10 months after the start of the study. If the gallbladder cannot be visualized on X-rays or in cases of calcification of stones, weak contractility of the gallbladder or frequent attacks of colic, Ursodez® should not be used.

In the treatment of patients in the late stages of primary biliary cirrhosis: Cases of decompensation of cirrhosis of the liver were extremely rare. After discontinuation of therapy, there was a regression of decompensation symptoms.

Long-term therapy with high doses of Ursodeoxycholic acid (28-30 mg / kg / day) can lead to serious side effects in patients with primary sclerosing cholangitis.

In patients with diarrhea, the dosage of the drug should be reduced. If persistent diarrhea occurs, treatment should be discontinued.

Influence on the ability to drive motor vehicles and manage mechanisms

The effect on the ability to drive vehicles and mechanisms was not revealed.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of reach of children.

Active ingredient

Ursodeoxycholic acid

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Purpose

For adults as directed by your doctor

Indications

Cholelithiasis, Cirrhosis of the liver