Ursodeoxycholic acid - instructions for use, dose, side effects, contraindications

Inhibition of the synthesis and secretion of cholesterol by the liver, inhibition of its absorption from the digestive tract, leaching of cholesterol from the biliary calculi with their dissolution. Pharmacological effects: cholelitholytic - dissolution of cholesterol (roentgenogenous) concrements of the gallbladder.

Pharmacokinetics:

Bioavailability of 90%. The connection with plasma proteins is high. Biotransformation in the liver into taurine and glycine conjugates. Half-life 100 h. Elimination with feces (50-70%), intestinal-hepatic circulation.

Indications:Cholesterol gallstones in the gallbladder and common bile duct in patients when surgical or endoscopic treatment can not be performed. Cholesterol stones of the gallbladder and common bile duct no more than 1.5-2 cm in diameter 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.Acute hepatitis, cystic fibrosis of the liver, congenital atresia of the bile duct. Biliary reflux-esophagitis and gastritis. Biliary Dyspeptic syndrome in cholecystopathy and dyskinesia of bile ducts. Prevention and treatment of cholestatic syndrome caused by the intake of hormonal contraceptives. For the normalization of liver function in patients receiving therapy with cytostatics, as well as in patients with alcoholic liver damage. Transplantation of the liver and other organs (auxiliary treatment).

ICD-10

IV.E70-E90.E84.9 Cystic fibrosis, unspecified

IV.E70-E90.E84.8 Cystic fibrosis with other manifestations

IV.E70-E90.E84.1 Cystic fibrosis with intestinal manifestations

IV.E70-E90.E84.0 Cystic fibrosis with pulmonary manifestations

IV.E70-E90.E84 Cystic fibrosis

XI.K20-K31.K21.0 Gastroesophageal reflux with esophagitis

XI.K20-K31.K20 Esophagitis

XVII.Q38-Q45.Q44.6 Cystic liver disease

XI.K70-K77.K76.9 Liver disease, unspecified

XI.K70-K77.K76.5 Venoocclusive liver disease

XI.K70-K77.K75.9 Inflammatory liver disease, unspecified

XI.K70-K77.K70.9 Alcoholic liver disease, unspecified

XI.K70-K77.K70 Alcoholic liver disease

XI.K70-K77.K71.8 Toxic liver damage with a picture of other liver disorders

XI.K70-K77.K71.7 Toxic liver damage with fibrosis and liver cirrhosis

XI.K70-K77.K77.0 * Liver disorders in infectious and parasitic diseases classified elsewhere

XI.K70-K77.K77 * Liver disorders in diseases classified elsewhere

XI.K70-K77.K71.9 Toxic liver disease, unspecified

XI.K70-K77.K71.6 Toxic liver damage with a picture of hepatitis, not elsewhere classified

XI.K70-K77.K71.5 Toxic liver damage, proceeding according to the type of chronic active hepatitis

XI.K70-K77.K71.4 Toxic liver damage, proceeding according to the type of chronic lobular hepatitis

XI.K70-K77.K71.3 Toxic liver damage, proceeding according to the type of chronic persistent hepatitis

XI.K70-K77.K71.2 Toxic liver damage, proceeding according to the type of acute hepatitis

XI.K70-K77.K71.1 Toxic liver damage with hepatic necrosis

XI.K70-K77.K71.0 Toxic liver damage with cholestasis

XI.K70-K77.K71 Toxic liver disease

XI.K80-K87.K80.5 Stones of the bile duct without cholangitis or cholecystitis

XI.K80-K87.K80.4 Stones of the bile duct with cholecystitis

XI.K80-K87.K80.3 Stones of the bile duct with cholangitis

XI.K80-K87.K80.2 Stones of the gallbladder without cholecystitis

XI.K80-K87.K80.1 Stones of the gallbladder with other cholecystitis

XI.K80-K87.K80.0 Stones of the gallbladder with acute cholecystitis

Contraindications:

Hypersensitivity, acute inflammatory diseases of the gallbladder, bile ducts and intestines, complete obstruction of the biliary tract, calcified gallstones, cirrhosis of the liver in the stage of decompensation, pronounced impairment of kidney function, pancreas.

Carefully:

Elderly age, renal and hepatic insufficiency, children under 18, pregnancy, breast-feeding.

Pregnancy and lactation:

FDA recommendation category B.

Adequate and well-controlled studies in humans have not been conducted. 4 women unintentionally received at therapeutic dose ursodeoxycholic acid in the first trimester, which did not lead to any negative effects on the fetus and the newborn. In studies on rats when administered at a dose exceeding the human dose 20 to 100 times, and on rabbits in a dose exceeding the dose for a person 5 times, it was not found that ursodeoxycholic acid causes side effects in the fetus. Nevertheless, it can not be ruled out that for a person ursodeoxycholic acid can be dangerous. Use with caution. There is no information on the penetration into breast milk. Use with caution.

Dosing and Administration:

The dosage regimen is set individually. Usually used in a dose of up to 10 mg / kg / day. The daily dose is taken once in the evening. The duration of treatment depends on the indications.

Side effects:

Perhaps: a transient increase in hepatic transaminase activity, skin itching, allergic reactions.

Rarely: diarrhea, calcification biliary stones.

Overdose:

Diarrhea.

Treatment is symptomatic.

Interaction:

With simultaneous use with cyclosporin, absorption improves unpredictably and the concentration of cyclosporin in the blood plasma increases.

A case of a decrease in the concentration of ciprofloxacin in the blood plasma in a patient receiving ursodeoxycholic acid is described.

Special instructions:

For successful litholysis with ursodeoxycholic acid, the following conditions must be met: stones must be pure cholesterol, i.e. not to give a shadow on the roentgenogram; The size of the stones should not exceed 15-20 mm; the gallbladder must fully retain its function; The gallbladder should be filled with stones no more than half; the permeability of the cystic duct must be preserved; the common bile duct should be free of stones.

When ursodeoxycholic acid is used 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 at intervals of 3 months.

To monitor the effectiveness of treatment, it is recommended to perform X-ray and ultrasound examination of the bile ducts every 6 months.

To prevent the recurrence of cholelithiasis, treatment should continue for several more months after the dissolution of gallstones.

Instructions

Ursodeoxycholic acid (Acidum ursodeoxycholicum)