Ursosan

Ursosan helps reduce the production of cholesterol in the liver, as well as its absorption through the intestines. In addition, due to the formation of liquid complexes with cholesterol, this drug reduces the number of cholesterol stones formed in the body and helps dissolve them.

Indications Ursosan

The drug is prescribed in case of occurrence of cholesterol radiopaque stones in the gallbladder (under conditions of normal functioning of this organ, as well as with a maximum size of 15 mm in diameter). The drug is also used in case of gastritis with concomitant bile reflux. Ursosan can be prescribed for symptomatic treatment of primary biliary cirrhosis of the liver (if there is no decompensated form of the disease).

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Release form

Ursosan is available in capsules. One blister pack contains 10 capsules. 1 pack may contain 1, 5 or 10 blisters.

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Pharmacodynamics

The drug is hepatoprotective - it protects liver function - and in addition, it has cholelitholytic, choleretic, as well as hypocholesterolemic and hypolipidemic effects. In addition, it also performs some immunomodulatory functions.

Since ursodeoxycholic acid has strong polar properties, it is able to integrate into the membrane of cells and tissues of the gastrointestinal tract (such as cholangiocytes, hepatocytes, and epithelial cells), normalize their structure, and protect against bile salts that have a toxic effect - reduce their cytotoxic effect. It also creates non-toxic mixed micelles in combination with bile acid, thereby reducing the ability of gastric contents to destroy membrane cells in diseases such as biliary reflux esophagitis. In addition, UDCA stimulates choleresis, that is, the secretion of bile by hepatocytes (simultaneously reducing its concentration), which contains many bicarbonates, thereby eliminating intrahepatic cholestasis. In cholestasis, this acid activates alpha-protease (Ca2+-dependent) and also promotes exocytosis, reducing the elevated concentration of bile acids of a toxic nature (such as deoxycholic, chenodeoxycholic, and lithocholic) due to chronic disorders in liver function.

In the intestine, the amount of absorbed lipophilic acids decreases, their fractional turnover increases during portal-biliary circulation, and choleresis is induced, during which bile passage occurs with the removal of bile acid from the body through the intestine. By suppressing intestinal absorption of cholesterol together with its synthesis in the liver, and in addition, by reducing its secretion into bile, the level of saturation with this substance decreases. The solubility indices of cholesterol increase, resulting in the appearance of liquid crystals. The level of the lithogenic index of bile decreases, and at the same time the saturation index of bile acid increases, as a result of which the process of pancreatic and gastric secretion increases, and the activity of lipase production increases. Since the cholesterol level becomes lower, it is better excreted from stones, and as a result, they dissolve better. In this way, the possibility of the formation of new stones in the hepatobiliary system is prevented.

The immunomodulatory effect of the drug is achieved by suppressing the expression of histocompatibility antigens (in the walls of hepatocytes (type HLA-1), as well as cholanocytes (type HLA-2)), stabilizing the activity of NK/T-lymphocytes, reducing the number of eosinophils, producing IL-2, and suppressing immunocompetent cells (primarily IgM). The process of fibrosis development is delayed.

Pharmacokinetics

UDCA is absorbed through the small intestine by passive transport (approximately 90%), and through the ileum by active transport. It reaches the maximum possible concentration after 1-3 hours. After oral administration of 50 mg, after half an hour/1 hour/1.5 hours, the values are 3.8/5.5/3.7 mmol/l, respectively. The time to reach the maximum possible concentration is 1-3 hours. It binds to plasma proteins by 96-99%. It passes through the placental barrier. If Ursosan is taken systematically, UDC acid will become the main bile acid in the blood serum. When broken down in the liver, it is converted into taurine conjugate and salicyluric acid, after which these elements are excreted into bile. About 50-70% of the drug is excreted with it. The remainder of the unabsorbed UDCA enters the large intestine, where it is broken down by bacteria (in the process of 7-dehydroxylation). The resulting lithocholic acid is fragmentarily absorbed from the large intestine and sulfated through the liver, after which it is excreted as a sulfolithocholyl taurine or sulfolithocholyl glycine compound.

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Dosing and administration

The drug is taken orally, it is not recommended to chew or crush the capsules in any other way before taking. Usually the daily dose is taken at one time - it is best to take it before bedtime, while washing it down with water. The dosage, as well as the duration of the treatment course, should be determined by the attending physician.

If the patient has cholesterol gallstones, the daily dosage is usually calculated at 10 mg of the drug per 1 kg of weight. The course of treatment lasts from six months to 2 years, but if no improvements (reduction in the size of the stones) are observed within the first year after starting to take the drug, the therapy should be discontinued.

At the initial stage of treatment, it is necessary to check the activity of liver transaminases every month. It is also necessary to monitor changes in the size of stones - by means of cholecystography or ultrasound (at least once every six months). In addition, during therapy, it is necessary to perform examinations in order to be able to detect the onset of calcification of stones in time (if calcified stones are found in the gallbladder, treatment with Ursosan is stopped).

For chemical-toxic reflux gastritis (C), the drug is usually prescribed in a dosage of 1 capsule/day. The therapeutic course usually lasts 10-14 days.

In case of PBC of the liver, the dosage of the drug is usually 14 mg/1 kg of weight per day. At the initial stage of treatment, the daily dose is divided into 3 separate doses (since it is not possible to divide the dose equally, because 1 capsule of the drug contains 250 mg of UDCA, it is recommended to drink most of the medicine in the evening).

The treatment course using Ursosan for PBC of the liver can have an unlimited duration. Sometimes at the initial stage of treatment, the clinical manifestations of the disease worsen - if this happens, the daily dose of the drug should be reduced to 1 capsule, gradually increasing it to the required amount (add 1 capsule each new week).

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Use Ursosan during pregnancy

The drug should not be taken in the 1st trimester of pregnancy. Ursosan can be prescribed in the 2nd or 3rd trimester, but only for vital indications. Before starting treatment with UDCA, a woman of childbearing age must completely eliminate the risk of pregnancy during the therapy period, using reliable contraceptive methods.

Contraindications

Ursosan is contraindicated in case of hypersensitivity to UDCA, as well as additional elements of the capsules.

The drug is not prescribed if the patient has inflammation of the gallbladder or its ducts (in acute form), blockage of the bile ducts or problems with the contractility of the gallbladder.

The drug is not used to treat patients with biliary colic, calcified gallstones, or those whose gallbladder cannot be visualized by radiological methods.

Contraindications include liver and kidney dysfunction, as well as children under 5 years of age.

Should be taken with caution by patients with the following diseases: ulcers, hepatitis or cirrhosis of the liver, extrahepatic cholestasis, as well as inflammatory processes in the intestines.

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Side effects Ursosan

Side effects of the drug Ursosan include:

Gastrointestinal organs, as well as the hepatobiliary system: pain in the liver (usually occurs in people with PBC of the liver), diarrhea, transient increase in transaminase activity, calcification of gallstones, and vomiting. In patients suffering from PBC, liver cirrhosis may progress to a decompensated stage with partial progression after completion of treatment.

Urticaria may occur at the beginning of treatment.

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Overdose

Overdose of Ursosan causes diarrhea. There is no specific medicine to treat this symptom – if an overdose occurs, the dose of the drug should be reduced. If this does not help to get rid of the discomfort, you should stop taking the medicine and perform procedures that restore the balance of water and salt in the body.

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Interactions with other drugs

Taking the drug in combination with cholestyramine, colestipol, and antacids (which contain substances such as aluminum oxide and hydroxide, and magnesium silicate) may reduce the absorption of UDCA. If these drugs must be taken together, they should be taken at least 2 hours apart.

When taken simultaneously with cyclosporine, the intestinal absorption of this substance increases. Therefore, it is necessary to carefully monitor the amount of cyclosporine in the plasma and adjust its dosage if necessary.

A decrease in the absorption rates of ciprofloxacin may be observed if it is taken in combination with UDCA.

Ursosan stimulates the production of cytochrome P450 3A and is also capable of changing the concentration of drugs metabolized by this enzyme in plasma. When combining this drug with dapsone and nitrendipine, the dosage of the latter should be monitored.

When taken simultaneously with probucol, clofibrate, and bezafibrate, the effectiveness of treatment using UDCA is reduced.

The effectiveness of Ursosan is reduced if taken in combination with estrogens and oral contraceptives. In addition, its effect is reduced if the drug is taken by a patient who is on a diet with high cholesterol levels and, conversely, low fiber levels.

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Storage conditions

The medicine must be stored at a temperature of 15-25 °C.

Shelf life

Ursosan is approved for use for 4 years from the date of manufacture.