Dissolution of cholesterol gallstones with a diameter not exceeding 15 mm, permeable to X-rays, in patients who, despite the presence of stones, gallbladder function is preserved. Symptomatic treatment of primary biliary cirrhosis of the liver, provided that no decompensated cirrhosis is present.
Composition:
1 tabl contains 250 mg of ursodeoxycholic acid.
Action:
Following oral administration of ursodeoskycholic acid, the saturation of bile cholesterol decreases as a result of inhibiting the absorption of cholesterol in the intestine and reducing the secretion of cholesterol into the bile. Cholesterol deposits gradually dissolve, probably as a result of cholesterol scattering and the formation of liquid crystals. The action of ursodeoskycholic acid in diseases of the liver and bile ducts consists in the replacement of lipophilic, detergent-like, toxic bile acids hydrophilic and nontoxic ursodeoskycholic acid with cytoprotective properties, improving the secretory function of hepatocytes and regulating immunological processes. After oral administration, ursodeosycholic acid is rapidly absorbed. 60-80% of the administered dose is absorbed. Absorbed ursodeoskycholic acid is almost entirely conjugated in the liver with amino acids Glycine and Taurine, and then secreted into the bile. Approx. 60% of the drug is metabolised during the first pass through the liver. The portion of ursodeoskycholic acid is broken down by intestinal bacteria into 7-ketolitocholic acid and lithocholic acid, which acts hepatotoxically in animals. In humans, a very small amount of lithocholic acid is absorbed. After absorption, it is detoxified by sulphurisation in the liver, then it is secreted into the bile and finally excreted in the faeces. T0,5 Ursodeoskycholic acid is 3.5-5.8 days.
Contraindications:
Hypersensitivity to the active substance and / or excipients. acute inflammation of the gall bladder and bile ducts. Obstruction of the common bile duct or the follicular duct. It should not be used if the gallbladder is invisible on the X-ray, if calcifications occur in the deposits, if the gallbladder contractile function is disturbed or if the bile colic often occurs.
Precautions:
The parameters of liver function (AST, ALT and GGT) should be checked every 4 weeks for the first 3 months of treatment, and then every 3 months. To assess the effectiveness of treatment and early detection of calcifications within the bile deposit, radiological examination of the gallbladder should be performed ( oral cholecystography) after 6-10 months from 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).
Pregnancy and lactation:
The preparation should not be used during the first trimester of pregnancy. Women of childbearing age should use effective contraception during treatment. Pregnancy must be ruled out before starting treatment. It should not be used during breast-feeding.
Side effects:
Common: bright stools, diarrhea. Very rare: calcification of gallstones, urticaria. Very rarely during the treatment of primary biliary cirrhosis: severe pain in the right upper abdominal quadrant, worsening of the symptoms of liver disease (which partially resolved after discontinuation of the drug).
Dosage:
Orally. Dissolving of gallstones: 8-10 mg / kg daily in 2 doses. The following dosage regimen is recommended: patients with mc. up to 60 kg: 500 mg a day (2 tables in the evening); patients with mc. 60-80 kg: 750 mg daily (1 morning table and 2 evening table); patients with mc. 80-100 kg: 1000 mg daily (1 morning table and 3 evening tables); patients with mc. above 100 kg: 1250 mg per day (2 morning tables and 3 evening tables). Primary biliary cirrhosis: 5-10 mg / kg daily, once or in two divided doses.