Pharmachologic effect
Hepatoprotector. Ursodeoxycholic acid is a bile acid. Reduces cholesterol in bile mainly by dispersing cholesterol and forming a liquid crystalline phase. It affects the enterohepatic circulation of bile salts, reducing the reabsorption in the intestines of endogenous, more hydrophobic and potentially toxic compounds.
In vitro studies have shown that ursodeoxycholic acid has a direct hepatoprotective effect and reduces the hepatotoxicity of hydrophobic bile salts.
It has an effect on immunological reactions, reducing the pathological expression of class I HLA antigens on hepatocytes and inhibiting the production of cytokines and interleukins.
Ursodeoxycholic acid reduces the lithogenic index of bile, increasing the content of bile acids in it. Promotes partial or complete dissolution of cholesterol gallstones when taken orally. It has a choleretic effect.
Indications of the active substances of the drug Ursodeoxycholic acid
Cholesterol gallstones in the gallbladder and common bile duct in patients when treatment with a surgical or endoscopic method is impossible. Cholesterol stones of the gallbladder and common bile duct with a diameter of not more than 1.5-2 cm after extracorporeal lithotripsy or mechanical lithotripsy. Primary biliary cirrhosis (before the formation of advanced fibrosis and cirrhosis of the liver). Chronic active hepatitis with cholestatic syndrome.
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Acute hepatitis, cystic fibrosis of the liver, congenital atresia of the bile duct. Biliary reflux esophagitis and gastritis. Biliary dyspeptic syndrome with cholecystopathy and biliary dyskinesia. Prevention and treatment of cholestatic syndrome due to the use of hormonal contraceptives. To normalize liver function in patients receiving cytostatic therapy, as well as in patients with alcoholic liver damage. Transplantation of the liver and other organs (auxiliary treatment).
Side effect
Perhaps: a transient increase in the activity of hepatic transaminases, skin itching, allergic reactions.
Rarely: diarrhea, calcification of gallstones.
Contraindications
Acute inflammatory diseases of the gallbladder and biliary tract, liver cirrhosis in the stage of vascular and parenchymal decompensation and / or pronounced activity, ULC, Crohn's disease, severe renal impairment, increased sensitivity to ursodeoxycholic acid.
Pregnancy and lactation
Ursodeoxycholic acid should not be used during pregnancy.
Women of childbearing age during the treatment with ursodeoxycholic acid are recommended to use non-hormonal contraceptives or contraceptives with a low estrogen content.
It is not known whether ursodeoxycholic acid is excreted in breast milk.
Use for impaired liver function
Contraindicated in cirrhosis of the liver in the stage of vascular and parenchymal decompensation and / or marked activity.
Use for impaired renal function
Contraindicated in severe renal impairment.
Special instructions
For successful litholysis using ursodeoxycholic acid, the following conditions must be met: the stones must be pure cholesterol, i.e. do not give a shadow on the radiograph; the size of the stones should not exceed 15-20 mm; the gallbladder must fully retain its function; the gall bladder should be filled with stones no more than half; patency of the cystic duct should be maintained; the common bile duct should be free of stones.
When using ursodeoxycholic acid to dissolve gallstones in the first 3 months of treatment, it is necessary to determine the activity of liver transaminases every 4 weeks. In the future, these studies can be carried out with an interval of 3 months.
To monitor the effectiveness of treatment, it is recommended that an X-ray and ultrasound examination of the biliary tract be performed every 6 months.
For the prevention of recurrence of cholelithiasis, treatment should be continued for several months after the dissolution of gallstones.
Drug interaction
With simultaneous use with cyclosporine, absorption increases unpredictably and the concentration of cyclosporin in the blood plasma increases.
A case of a decrease in the concentration of ciprofloxacin in blood plasma in a patient receiving ursodeoxycholic acid is described.