URSEL-LM [Ursodeoxycholic acid] 250 mg Capsules

instructions for the medical use of a medicinal product

URSEL-LM

Tradename

Ursel-LM, Урсел-LM

International non-proprietary name or generic name

Ursodeoxycholic acid, Урсодезоксихолевая кислота

Dosage form

Capsules.

Composition

Each capsule contains:

active substance: ursodeoxycholic acid BP 250 mg;

excipients: starch, aerosil 200, magnesium stearate.

Pharmacotherapeutic group

Hepatoprotector, cholelitholytic agent.

Code АТХ: А05АА02

Pharmacological properties

Pharmacodynamics

Hepatoprotective agent, also has choleretic, cholelitholytic, hypolipidemic, hypocholesterolemic and some immunomodulatory effects. Possessing high polar properties, ursodeoxycholic acid (UDCA) is embedded in the membrane of hepatocytes, cholangiocytes and epithelial cells of the gastrointestinal tract, stabilizes its structure and protects the cell from the damaging effect of salts of toxic bile acids, thereby reducing their cytotoxic effect. Forms non-toxic mixed micelles with apolar (toxic) bile acids, which reduces the ability of gastric refluxate to damage cell membranes in biliary reflux gastritis and reflux esophagitis. By reducing the concentration and stimulating choleresis, rich in bicarbonates, UDCA effectively promotes the resolution of intrahepatic cholestasis. In cholestasis, it activates Ca2+-dependent alpha-protease and stimulates exocytosis, reduces the concentration of toxic bile acids (chenodeoxycholic, lithocholic, deoxycholic, etc.), the concentrations of which are increased in patients with chronic liver diseases. Competitively reduces the absorption of lipophilic bile acids in the intestine, increases their "fractional" turnover during enterohepatic circulation, induces choleresis, stimulates the passage of bile and the excretion of toxic bile acids through the intestine. Reduces the saturation of bile with cholesterol by inhibiting its absorption in the intestine, suppressing synthesis in the liver and decreasing secretion into bile; increases the solubility of cholesterol in bile, forming liquid crystals with it; reduces the lithogenic index of bile, increases the concentration of bile acids in it, causes increased gastric and pancreatic secretion, enhances lipase activity, and has a hypoglycemic effect. Causes partial or complete dissolution of cholesterol gallstones, reduces the saturation of bile with cholesterol, which promotes its mobilization from gallstones. The result is the dissolution of cholesterol gallstones and prevention of the formation of new stones. The immunomodulatory effect is due to the inhibition of the expression of histocompatibility antigens - HLA-1 - on the membranes of hepatocytes and HLA-2 - on cholangiocytes, normalization of the natural killer activity of lymphocytes, the formation of interleukin-2, a decrease in the number of eosinophils, suppression of immunocompetent immunoglobulins (Ig), primarily IgM. Delays the progression of fibrosis. Regulates the processes of apoptosis of hepatocytes, cholangiocytes and epithelial cells of the gastrointestinal tract.

Pharmacokinetics

Ursodeoxycholic acid is absorbed in the small intestine by passive diffusion (about 90%), and in the ileum by active transport. The maximum concentration in blood plasma (Cmax) after oral administration of 50 mg after 30, 60, 90 minutes is 3.8 mmol / l, 5.5 mmol / l and 3.7 mmol / l, respectively. The time to reach the maximum concentration in plasma (TCmax) is achieved in 1-3 hours. The connection with plasma proteins is high - up to 96-99%. Penetrates the placental barrier. With systematic administration of the drug, ursodeoxycholic acid becomes the main bile acid in the blood serum. It is metabolized in the liver (clearance during the "first pass" through the liver) into taurine and glycine conjugates. The resulting conjugates are secreted into bile. About 50-70% of the total dose of the drug is excreted in bile. A small amount of unabsorbed ursodeoxycholic acid enters the colon, where it is broken down by bacteria (7-dehydroxylation); the resulting lithocholic acid is partially absorbed from the colon, but is sulfated in the liver and rapidly excreted as a sulfolithocholylglycine or sulfolithocholyltaurine conjugate.

Indications for use

- cholelithiasis (CSD): biliary sludge; dissolution of cholesterol gallstones in a functioning gallbladder in patients with high surgical risk and in patients after lithotripsy. The condition for successful treatment is a functioning gallbladder and the presence of pure radiotransparent cholesterol stones, the diameter of which does not exceed 2 cm, prevention of recurrence of stone formation after cholecystectomy.

- primary biliary cirrhosis stage I and II;

- primary sclerosing cholangitis;

- hepatitis (chronic and acute viral, atypical forms of chronic autoimmune);

- non-alcoholic fatty liver disease, non-alcoholic steatohepatitis;

- toxic liver damage (including alcoholic, drug-induced);

- biliary dyspepsia;

- bile reflux gastritis and esophagitis;

- cystic fibrosis;

- biliary dyskinesia;

- chronic opisthorchiasis.

Contraindications

- in individuals with hypersensitivity to the active or auxiliary substance of the drug;

- in patients with inflammatory diseases of the gallbladder and bile ducts in the acute period;

- in case of obstruction of the bile ducts;

- in case of liver cirrhosis in the decompensation stage;

- in case of inflammation of the intestine, Crohn's disease;

- in case of impaired renal and hepatic function;

- in children under 3 years of age in this dosage form.

Method of administration and dosage

Orally. The capsules should be taken regularly, without chewing, with a small amount of liquid.

Dissolution of cholesterol gallstones

The recommended dose of ursodeoxycholic acid depends on body weight and is 10 mg/kg/day.

Calculation of the daily amount of Ursel-LM capsules depending on body weight:

• Body weight up to 60 kg - 2 capsules;

• Body weight 61-80 kg - 3 capsules;

• Body weight 81-100 kg - 4 capsules;

• Body weight over 100 kg - 5 capsules.

The drug Ursel-LM should be taken daily in the evening, before going to bed (the capsules are not chewed), 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 stones have dissolved.

Biliary reflux gastritis and reflux esophagitis

1 capsule of the drug daily in the evening, before bedtime (the capsules are not chewed), 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.

Primary biliary cirrhosis (symptomatic treatment)

The daily dose depends on body weight and ranges from 3 to 7 capsules (approximately 14±2 mg/kg ursodeoxycholic acid).

During the first 3 months of treatment, the use of Ursel-LM should be divided into several doses during the day. After improvement of liver parameters, the daily dose of the drug can be taken once in the evening.

The following regimen for using the drug is recommended

The use of Ursel-LM acid for the treatment of primary biliary cirrhosis can be continued indefinitely. In patients with primary biliary cirrhosis, clinical symptoms may rarely worsen at the beginning of treatment, for example, itching may become more frequent. In this case, treatment should be continued by taking 1 capsule daily, then the dosage should be gradually increased (increasing the daily dose by 1 capsule weekly) until the recommended dosage regimen is again reached.

Primary sclerosing cholangitis

12-15 mg/kg/day (up to 20 mg/kg/day) for 6-24 months (up to several years).

Cystic fibrosis of the liver

The daily dose is 12-15 mg/kg, if necessary the dose can be increased to 20-30 mg/kg/ 2-3 doses per day for 6-24 months or more.

Chronic hepatitis of various origins, non-alcoholic steatohepatitis, alcoholic liver disease, acute hepatitis and toxic liver damage

The daily dose is 12-15 mg/kg (2-5 capsules in 2-3 doses), the duration of therapy is 6-12 months or more.

Dyskinesia of the biliary tract

Average daily dose is 10 mg/kg in 2 doses for 2 weeks to 2 months.

For children over 3 years of age, the drug is prescribed individually, based on the calculation of 20 mg/kg/day.

Special instructions and precautions

Before using the drug, consult a doctor.

When taking the drug to dissolve gallstones, the following conditions must be met: the stones must be cholesterol (radionegative), their size should not exceed 15-20 mm, the gallbladder must remain functional and be filled with stones no more than half, the patency of the cystic and common bile ducts must be maintained.

With long-term (more than 1 month) use of the drug, every 4 weeks in the first 3 months of treatment, then every 3 months, a biochemical blood test should be performed to determine the activity of liver transaminases. The effectiveness of treatment should be monitored every 6 months using ultrasound data of the biliary tract. After complete dissolution of the stones, it is recommended to continue using the drug for at least 3 months in order to promote the dissolution of the remaining stones, the size of which is too small to detect, and to prevent recurrence of stone formation.

The drug is not recommended for use in cases where frequent biliary colic is noted, as well as if the preservation of the excretory functions of the gallbladder has not been proven.

It is not prescribed to children under 3 years of age due to the complexity of dosing.

Application during pregnancy and during breastfeeding

Use during pregnancy is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

If use during lactation is necessary, breastfeeding should be discontinued.

Side effect

Ursel-LM is well tolerated by patients. Side effects that may occur when taking the drug are not serious enough. Possible diarrhea (may be dose-dependent) self-limiting, sometimes skin itching. Rarely - calcification of gallstones, transient (transient) increase in the activity of liver transaminases, nausea, vomiting, abdominal pain, allergic reactions.

If any of the side effects listed in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.

Interaction with other medicinal products

The effectiveness of Ursel-LM may be reduced by concomitant administration of other medications, mainly drugs that reduce gastric acidity/antacids/containing aluminum hydroxide, as well as drugs containing cholestyramine, cholesterol. If concomitant treatment with the above-mentioned drugs is necessary, it is recommended to use them 2 hours before or after taking Ursel-LM. Ursodeoxycholic acid may increase intestinal absorption of cyclosporine. Therefore, it is necessary to monitor cyclosporine levels and adjust the doses of cyclosporine in people taking this drug concomitantly. Antacids containing aluminum and ion exchange resins (colestyramine) reduce absorption. Lipid-lowering drugs (especially clofibrate), estrogens, neomycin or progestins increase bile saturation with cholesterol and may reduce the ability to dissolve cholesterol gallstones. Your doctor should be informed about all medications that you are currently taking or will start taking.

Overdose

Symptoms: Diarrhea may occur.

Treatment: Symptomatic treatment, restoration of fluid and electrolyte balance.

Storage conditions

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

Keep out of reach of children.

Shelf life

3 years. Do not use after the expiration date stated on the package.

Vacation conditions

Dispensed by prescription.

Release form

10 tablets in an aluminum foil blister. 1 blister together with instructions for use in a cardboard box.