Dissolution of cholesterol stones in the gall bladder in patients with contraindications for surgical treatment - the diameter of the stones can not exceed 15 mm, deposits must be permeable to X-rays (no shadows in the X-ray - cholecystography), gallbladder function should be maintained despite the presence stones. Symptomatic treatment of primary biliary cirrhosis (PBC), provided that no decompensated cirrhosis is present.
Ursodeoxycholic acid is a natural bile acid found in small amounts in human bile. After oral administration of ursodeoxycholic acid, the saturation of bile cholesterol decreases as a result of suppression of cholesterol absorption in the intestine and reduction of cholesterol secretion to bile. Cholesterol deposits gradually dissolve, probably as a result of cholesterol scattering and formation of liquid crystals. The action of ursodeoxycholic acid in diseases of the liver and bile ducts consists in replacing lipophilic, detergent-like, toxic bile acids by hydrophilic and nontoxic ursodeoxycholic acid with cytoprotective properties, improving the secretory function of hepatocytes and regulating immunological processes. After oral administration, ursodeoxycholic acid is rapidly absorbed in the small intestine, 60-80% of the dose is absorbed. Absorbed ursodeoxycholic acid is almost entirely conjugated in the liver with amino acids, Glycine and Taurine, and then secreted into the bile. Approx. 60% of ursodeoxycholic acid is metabolised during the first pass through the liver. Depending on the daily dose, the dysfunction and the condition of the liver, there is an increase in accumulation (accumulation) of hydrophilic ursodeoxycholic acid in the bile and at the same time a relative reduction in the amount of other more lipophilic bile acids. The portion of ursodeoxycholic acid is broken down by intestinal bacteria to 7-ketolithiol acid and lithocholic acid. Lithocholic acid works hepatotoxically and causes damage to the liver parenchyma in animals of many species. In humans, a very small amount of lithocholic acid is absorbed. After absorption, it is detoxified by sulphurization in the liver, then it is secreted into the bile and eventually excreted in the faeces. T0,5 Ursodeoxycholic acid is 3.5 - 5.8 days.
Contraindications:
Hypersensitivity to bile acids or any of the excipients. acute inflammation of the gall bladder and bile ducts. Obstruction of bile ducts (obstruction of the common bile duct or alveolar duct). Frequent episodes of biliary colic. Calcified gallstones visible in X-rays. Weakened gallbladder contractility.
Precautions:
The functional parameters of the liver should be monitored: AST, ALT, GGT every 4 weeks for the first 3 months of treatment, and then every 3 months, which will allow identifying responders and non-responders to treatment for patients treated for primary liver cirrhosis and early detection of potential liver liver damage, especially in patients with advanced primary biliary cirrhosis. In order to evaluate the effectiveness of treatment and early detection of calcifications within the bile deposits, a radiological examination of the gall bladder (oral cholecystography) should be performed 6-10 months after the start of treatment, depending on the diameter of the deposits. Photographs (review and contrast administration) should be performed both in upright and supine position (ultrasound monitoring). The drug should not be used if the gallbladder is invisible on the X-ray, calcifications within the deposits are present, the gallbladder contractile function is disturbed or the bile colic often occurs. In the event of diarrhea, the dose should be reduced, and if persistent diarrhea should be discontinued.The sodium content of the oral suspension: 11.39 mg (0.50 mmol) of sodium per 1 scoop (up to 5 ml) should be taken into account for patients using a controlled sodium diet.
Pregnancy and lactation:
Do not use during pregnancy unless clearly necessary (animal studies have shown a risk of harm to the fetus during treatment at an early stage of pregnancy). Women of childbearing age should use effective contraception during treatment - use of non-hormonal or low-estrogen oral contraceptives is recommended. Patients taking the medicine for the purpose of dissolving gallstones should use non-hormonal methods because oral hormonal contraceptives may increase cholelithiasis. The drug should not be used during breastfeeding.
Side effects:
Common: light stools or diarrhea. Very rare: calcification of gallstones, urticaria. Very rarely during the treatment of primary biliary cirrhosis, there was severe pain in the right upper abdominal quadrant and cases of worsening liver disease symptoms, which partially resolved after discontinuation of therapy.
Dosage:
Orally.Dissolving of cholesterol gallstones: approx. 10 mg / kg / day, at bedtime. Gallbladders dissolve after 6-24 months. If the diameter of the deposits does not decrease within 12 months, the drug should be discontinued. The effectiveness of treatment should be assessed ultrasonographically or radiologically every 6 months. During subsequent visits, it should be checked whether the deposits have calcified. The presence of calcification is an indication to stop the use of the drug.Symptomatic treatment of primary biliary cirrhosis: about 12-16 mg / kg / day. During the first 3 months of treatment, the drug should be taken in divided doses, and when the functional parameters of the liver improve, the daily dose may be taken once a day, in the evening. There is no time limit in taking the drug in primary biliary cirrhosis. In patients with primary biliary cirrhosis, at the beginning of treatment, symptoms may increase (eg pruritus) - in this case, treatment should be continued at a reduced daily dose, and then the dose should be gradually increased (increasing the dose every week) until the recommended dose is achieved. dose.Way of giving. Kaps. or tabl. powl. should be swallowed whole with a small amount of liquid. The drug should be taken regularly.