Ursosan: therapeutic effects and new application possibilities. XXI International Congress “Hepatology Today”. Satellite symposium of the company PRO.MED.CS Praha as

Description of the dosage form

White, hard, opaque gelatin capsules. Capsule contents: white or almost white powder, or white or almost white powder with pieces of mass, or white or almost white powder, compressed in a column and disintegrating when pressed.

Pharmacokinetics

Ursodeoxycholic acid is absorbed in the small intestine by passive diffusion (about 90%), and in the ileum by active transport. Cmax is achieved after 1-3 hours and is 3.8 when taken orally 50 mg after 30, 60 and 90 minutes; 5.5 and 3.7 mmol/l, respectively. Plasma protein binding - up to 96-99%. Penetrates through the placental barrier.

With systematic use of the drug Ursosan, ursodeoxycholic acid becomes the main bile acid in the blood serum and accounts for about 48% of the total amount of bile acids in the blood. The therapeutic effect of the drug depends on the concentration of ursodeoxycholic acid in bile.

Metabolized in the liver into taurine and glycine conjugates, which are secreted into bile. About 50-70% of the total dose is excreted in bile. A small amount of unabsorbed ursodeoxycholic acid enters the large intestine, where it is broken down by bacteria (7-dehydroxylation); the resulting lithocholic acid is partially absorbed from the colon, sulfated in the liver and quickly excreted in the form of sulfolithocholylglycine or sulfolitocholyltaurine conjugate.

Pharmacodynamics

Possessing high polarity, ursodeoxycholic acid 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. In addition, ursodeoxycholic acid forms double molecules that can be included in cell membranes (hepatocytes, cholangiocytes, epithelial cells of the gastrointestinal tract), stabilize them and make them immune to the action of cytotoxic micelles - a cytoprotective, hepatoprotective effect.

By reducing the concentration of bile acids toxic to the liver cell and stimulating choleresis with a high content of bicarbonates, ursodeoxycholic acid helps resolve intrahepatic cholestasis - an anticholestatic effect. Reduces the saturation of bile with cholesterol by inhibiting its absorption in the intestine, suppressing synthesis in the liver and reducing secretion into bile - a hypocholesterolemic effect. Increases the solubility of cholesterol in bile, forming liquid crystals with it; reduces the lithogenic index of bile.

The result is the dissolution of cholesterol gallstones and the prevention of the formation of new stones - the litholytic effect. The immunomodulatory effect is due to inhibition of the expression of HLA-1 antigens on the membranes of hepatocytes and HLA-2 on cholangiocytes, normalization of the natural killer activity of lymphocytes, etc. Significantly delays the progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis and alcoholic steatohepatitis - antifibrotic effect; reduces the risk of developing varicose veins of the esophagus. Ursodeoxycholic acid regulates the processes of apoptosis (aging and cell death) that are disrupted in the pathology of the liver and other organs - an anti-apoptotic effect.

Composition and release form

Ursosan, the instructions for use indicate this, contains ursodeoxycholic acid. Today, hepoprotective drugs based on it are considered the most effective.

The medicine is produced in the form of gelatin capsules filled with a mixture of white powder and powder granules in an amount of 250 mg. You can purchase Ursosan in blister packs of 10 or 20 capsules. The medicine is also offered in polyethylene jars containing 10, 20, 50 or 100 capsules. Cardboard packages must contain instructions for use.

Indications for use of Ursosan

Ursosan is prescribed if:

• uncomplicated cholelithiasis: biliary sludge;
• dissolution of cholesterol gallstones in the gallbladder if it is impossible to remove them surgically or endoscopically; prevention of recurrent stone formation after cholecystectomy;
• chronic active hepatitis;
• acute hepatitis;
• toxic (including medicinal) liver damage;
• alcoholic liver disease;
• non-alcoholic steatohepatitis;
• primary biliary cirrhosis of the liver;
• primary sclerosing cholangitis;
• cystic fibrosis of the liver (cystic fibrosis);
• atresia of the intrahepatic biliary tract, congenital atresia of the bile duct;
• biliary dyskinesia;
• biliary reflux gastritis and reflux esophagitis;
• biliary dyspeptic syndrome (with cholecystopathy and biliary dyskinesia);
• prevention of liver damage when using hormonal contraceptives and cytostatics.

How to take Ursosan for liver prevention?

Taking ursodeoxycholic acid is indicated not only in the treatment of diseases of the hepatobiliary tract and gastrointestinal tract. Ursosan capsules are also recommended to be taken as a prophylactic agent in the following cases:

• to prevent the development of liver pathologies;
• to support the body during the labile course of liver diseases.

The drug is prescribed to both adults and young patients starting from the age of 3. Use during pregnancy and breastfeeding is assessed separately, weighing the possible benefits and potential risks for the child.

As a prophylactic agent, ursodeoxycholic acid is taken in long courses. The duration depends on the condition of the hepatobiliary tract and varies from a week to several years. The effectiveness of maintenance therapy depends on the stable resumption of the main active substance in the bloodstream, so continuous use of the medication is important.

Mode of application

Ursosan capsules are intended for oral administration. The drug compares favorably with other dosage forms by containing finely dispersed ursodeoxycholic acid, which is absorbed much faster. The active component of the drug is a synthetic analogue of tertiary bile acid and has a characteristic bitter taste, but it is successfully masked by the gelatin capsule shell.

When the shell dissolves, the bitter taste remains for a long time, so the capsules are swallowed whole, washed down with plenty of water.

If Ursosan is prescribed for preventive purposes, how to take it—before or after meals—depends on the activity of the gastrointestinal tract and hepatobiliary tract. It is not recommended to take the medicine on an empty stomach, so in the first half of the day it is taken only after meals. In the afternoon, it is permissible to divide the intake into two halves, consuming one part before meals, and the second after finishing the meal.

Contraindications for use

• hypersensitivity;
• X-ray positive (high calcium) gallstones;
• non-functioning gallbladder;
• bile-gastrointestinal fistula;
• acute cholecystitis;
• acute cholangitis;
• liver cirrhosis in the stage of decompensation;
• liver and/or kidney failure;
• obstruction of the biliary tract;
• acute infectious diseases of the gallbladder and bile ducts;
• empyema of the gallbladder.

Although Ursosan has no age restrictions for use, the drug capsules are used with caution in children aged 2 to 4 years due to possible difficulty in swallowing them.

Effect of the drug

According to the study, it has been proven that ursodeoxycholic acid is quickly absorbed in the intestine and is integrated into liver cells and provides them with protection from various negative factors, including toxic and alcohol damage. When taking the medicine, congestion in the organ decreases and the removal of acids accelerates.

Ursosan, the instructions for use emphasize this, has a choleretic effect. The active substance is capable of:

• Reduce cholesterol production in the liver and slow down its absorption in the intestines.
• Reduce the saturation of bile with cholesterol.
• Increase the content of bile acids.
• Increase the solubility of cholesterol in the biliary system.

Ursosan dosage

Ursosan is taken orally with a sufficient amount of water.

• Diffuse liver diseases, cholelithiasis (cholesterol gallstones and biliary sludge) - continuously for a long time (from several months to several years) in a daily dose of 10 to 12-15 mg/kg (2-5 caps.). For diffuse liver diseases, the daily dose of Ursosan is divided into 2-3 doses, the capsules are taken with food. For cholelithiasis, the entire daily dose of Ursosan is taken once at night. The duration of treatment for dissolving stones is until complete dissolution, plus another 3 months. for the prevention of recurrent stone formation.
• For biliary reflux gastritis and reflux esophagitis, Ursosan is taken 250 mg/day (1 capsule) before bedtime. The course of treatment is from 10–14 days to 6 months, if necessary – up to 2 years.
• After cholecystectomy, to prevent recurrent cholelithiasis, Ursosan is used at a dose of 250 mg 2 times a day for several months.
• Toxic, drug-induced liver damage, alcoholic liver disease and biliary atresia - 10-15 mg/kg/day in 2-3 doses. Duration of therapy is 6–12 months. and more.
• Primary biliary cirrhosis - 10-15 mg/kg/day (if necessary - up to 20 mg/kg) in 2-3 doses. The duration of therapy is from 6 months. up to several years.
• Primary sclerosing cholangitis - 12–15 mg/kg/day (up to 20 mg/kg) in 2–3 doses. The duration of therapy is from 6 months. up to several years.
• Non-alcoholic steatohepatitis - 13-15 mg/kg/day in 2-3 doses. The duration of therapy is from 6 months. up to several years.
• Cystic fibrosis - 20-30 mg/kg in 2-3 doses. The duration of therapy is from 6 months. up to several years or for life.

For children over 2 years of age, Ursosan is prescribed individually at a dose of 10–20 mg/kg/day.

Ursosan price, where to buy

This medicine can be bought in Ukraine, Belarus and Russia. How much this drug costs depends largely on the number of capsules in one package.

You can buy this product in Moscow and other Russian cities at the following prices:

• price of Ursosan 100 tablets (250 mg) - approximately 1,500 rubles;
• price of Ursosan 50 capsules – approximately 800 rubles;
• the price of a package of 10 capsules is approximately 200 rubles.

Average price of Ursosan in Ukraine:

• capsules of 50 pieces per package – approximately 600 hryvnia;
• capsules of 100 pieces per package - approximately 1000 hryvnia;
• capsules of 10 pieces per package - approximately 100 hryvnia.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

ZdravCity

• Ursosan capsules 250 mg 10 pcs. Pro.Med.Cs
  161 rub. order
• Ursosan forte tab. p.p.o. 500 mg 100 pcs. PRO.MED.CS Prague j.s.

  RUR 3,268 order

Pharmacy Dialogue

• Ursosan (caps. 250 mg No. 50) Pro.Med.Cs.

  840 rub. order

• Ursosan (caps. 250 mg No. 10) Pro.Med.Cs.

  160 rub. order

• Ursosan tablets 500 mg No. 100Pro.Med.Cs.

  RUB 3,049 order

• Ursosan (caps. 250 mg No. 50)ZiO-Zdorovye CJSC

  790 rub. order

• Ursosan (caps. 250 mg No. 100)ZiO-Zdorovye CJSC

  RUB 1,561 order

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Pharmacy24

• Ursosan 250 mg No. 100 capsules PRO.MED.CS Prague a.t., Czech Republic/ PRO.MED.CS Prague a.s., Czech Republic
  1022 UAH.order

PaniPharmacy

• Ursosan capsule Ursosan caps. 250 mg No. 50, PRO.MED.CS Prague

  610 UAH. order

• Ursosan capsule Ursosan caps. 250 mg No. 100, PRO.MED.CS Prague

  1048 UAH order

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Possible negative side effects

Ursosan can cause exacerbation of chronic pathologies of the body (for example, psoriasis). With increased sensitivity, skin lesions are likely to develop. Other possible negative effects:

• nausea and vomiting;
• alopecia;
• disruption of the digestive system (constipation, diarrhea);

• abdominal pain;
• back pain;
• increased activity of liver transaminases.

The occurrence of standard side effects is not a reason to stop taking tablets and capsules. But if allergic reactions occur, it is necessary to stop using the drug and consult your doctor to eliminate allergy symptoms and replace the medication with an analogue.

Analogs and prices for drugs in Russia

Similar medications can be selected depending on the individual characteristics of the patient. It is not recommended to select and replace on your own. Read in detail about Ursosan analogues

Ursofalk or Ursosan is more effective as a hepatoprotector - this question interests many patients. The drug is best selected depending on the individual characteristics of the patient. Urosfalk is sold in the form of capsules and suspensions, which expands the range of its therapeutic capabilities. But both drugs have high positive characteristics and patient reviews.

A hepatoprotector as part of complex therapy against diseases of internal organs is an important component, since it helps restore the structure of their structure and functionality. Ursosan is one of the most effective and harmless medicines.