Composition, form of production and packaging
Capsules hard gelatinous, white, opaque, size No. 0; the contents of the capsules are white or almost white powder, or a white or almost white powder with slices of mass, or a white or almost white powder compressed with a column and decomposing when pressed.
1 caps.
ursodeoxycholic acid * 250 mg
Excipients: corn starch, magnesium stearate, silicon dioxide colloid, titanium dioxide, gelatin.
* - a non - proprietary international name recommended by WHO, an international name ursodeoxycholic acid has been accepted in the Russian Federation.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (5) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
Hepatoprotector. It also has choleretic, cholelitholitic, hypolipidemic, hypocholesterolemic and some immunomodulating action.
Possessing high polar properties, ursodeoxycholic acid forms nontoxic mixed micelles with apolar (toxic) bile acids, which reduces the ability of gastric reflux to damage cell membranes with biliary reflux gastritis and reflux esophagitis. In addition, ursodeoxycholic acid forms double molecules that can be included in the composition of cellular membranes of hepatocytes, cholangiocytes, GIT epitheliocytes, stabilize them and make them immune to the action of cytotoxic micelles.
Reducing the concentration of toxic bile acid for hepatocytes and stimulating choleresis, rich in bicarbonates, ursodeoxycholic acid effectively promotes resolution of intrahepatic cholestasis. Reduces the saturation of bile with cholesterol due to inhibition of its absorption in the intestine, suppression of synthesis in the liver and a decrease in secretion in bile; increases the solubility of cholesterol in bile, forming with it liquid crystals; reduces the lithogenic bile index. The result is the dissolution of cholesterol gallstones and the prevention of the formation of new concrements.
Immunomodulating effect is caused by oppression of HLA-1 antigens expression on membranes of hepatocytes and HLA-2 on cholangiocytes, normalization of natural killer activity of lymphocytes, etc. Reliably delay the progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis and alcoholic steatohepatitis; reduces the risk of developing varicose veins of the esophagus. Ursodeoxycholic acid slows down the processes of premature aging and cell death (hepatocytes, cholangiocytes).
PHARMACOKINETICS
Suction and distribution
Ursodeoxycholic acid is absorbed from the small intestine due to passive diffusion (about 90%), and in the ileum through active transport. In this case, the concentration of ursodeoxycholic acid when taking the drug inside at a dose of 50 mg after 30, 60, 90 minutes is 3.8 mmol / l, 5.5 mmol / l and 3.7 mmol / l, respectively. C max is achieved in 1-3 hours.
Binding to plasma proteins is high - up to 96-99%. Penetrates through the placental barrier. With the systematic administration of Ursosan ursodeoxycholic acid becomes the main bile acid in the blood serum and accounts for about 48% of the total amount of bile acids in the blood. The therapeutic effect of the drug depends on the concentration of ursodeoxycholic acid in bile.
Metabolism and excretion
Metabolised in the liver (clearance during primary passage through the liver) into taurine and glycine conjugates. The resulting conjugates are secreted into bile. About 50-70% of the total dose of the drug is excreted with bile. A small amount of non-succinic ursodeoxycholic acid enters the large intestine, where it undergoes cleavage by bacteria (7-dehydroxylation); the resulting lithocholic acid is partially absorbed from the colon, but is sulfated in the liver and is rapidly excreted as a sulfolithocholylglycine or sulfolithocholyltaurine conjugate.
INDICATIONS
- uncomplicated cholelithiasis: biliary sludge; dissolution of cholesterol gallstones in the gallbladder, if they can not be removed by surgical or endoscopic methods;prevention of recurrence of stone formation after cholecystectomy;
- chronic active hepatitis;
acute hepatitis;
- toxic (including medicinal) liver damage;
- alcoholic liver disease;
- non-alcoholic steatohepatitis;
- primary biliary cirrhosis of the liver;
- primary sclerosing cholangitis;
- Cystic fibrosis (cystic fibrosis) of the liver;
- atresia of the intrahepatic biliary tract (including congenital atresia of the bile duct);
- biliary dyskinesia;
- biliary reflux gastritis and reflux esophagitis;
- biliary dyspeptic syndrome (with cholecystopathy and biliary dyskinesia);
- Prevention of liver damage with the use of hormonal contraceptives and cytostatics.
DOSING MODE
Capsules of Ursosana are taken orally by washing with a sufficient amount of water.
With diffuse liver disease, cholelithiasis (cholesterol gallstones and biliary sludge), the drug is prescribed continuously for a long time (from several months to several years) at a daily dose of 10 mg / kg body weight to 12-15 mg / kg (2- 5 caps.).
With diffuse liver diseases, the daily dose of Ursosana is divided into 2-3 doses, the capsules are taken with food.
With cholelithiasis, the whole daily intake is taken once for the night. The duration of taking the drug to dissolve the stones - until complete dissolution, and then another 3 months to prevent the recurrence of stone formation.
With biliary reflux gastritis and reflux esophagitis, the drug is prescribed 250 mg (1 caps.) Per day, before bedtime. The course of treatment - from 10-14 days to 6 months, if necessary - up to 2 years.
After cholecystectomy, for the prevention of recurrent cholelithiasis, the recommended dose is 250 mg 2 times / day for several months.
With toxic, medicinal liver damage, alcoholic liver disease and atresia of the biliary tract, the daily dose is established at the rate of 10-15 mg / kg / 2-3 times. The duration of therapy is 6-12 months or more.
In primary biliary cirrhosis the drug is prescribed at the rate of 10-15 mg / kg / day (if necessary - up to 20 mg / kg) in 2-3 divided doses. Duration of therapy is from 6 months to several years.
With the primary sclerosing cholangitis - 12-15 mg / kg / day (up to 20 mg / kg) in 2-3 divided doses. Duration of therapy is from 6 months to several years.
With non-alcoholic steatohepatitis - 13-15 mg / kg / day in 2-3 divided doses. Duration of therapy is from 6 months to several years.
In cystic fibrosis, the dose is set at a rate of 20-30 mg / kg / day in 2-3 doses. Duration of therapy is from 6 months to several years.
For children over the age of 2 years, the dose of the drug is set individually at the rate of 10-20 mg / kg / day.
SIDE EFFECT
On the part of the digestive system: nausea, vomiting, diarrhea (may be dose-dependent), constipation, transient (transient) increase in hepatic transaminase activity;rarely - calcification of gallstones.
Other: back pain, allergic reactions, exacerbation of previously existing psoriasis, alopecia; rarely - calcification of gallstones ..
CONTRAINDICATIONS
- X-ray positive (high in calcium) gallstones;
- non-functioning gallbladder;
- bile-gastrointestinal fistula;
- Acute cholecystitis;
- Acute cholangitis;
- cirrhosis of the liver in the stage of decompensation;
- liver failure;
- kidney failure;
- Obturation of the bile ducts;
- acute infectious diseases of the gallbladder and bile ducts;
- Empyema of the gallbladder;
- Hypersensitivity to the components of the drug.
With caution apply Ursosan in children aged 2 to 4 years, t. it may be difficult to swallow capsules, although ursodeoxycholic acid has no age limitation in use.
PREGNANCY AND LACTATION
The use of ursodeoxycholic acid in pregnancy is possible only if the expected benefit for the mother exceeds the potential risk for the fetus (adequate strictly controlled studies of the use of ursodeoxycholic acid in pregnant women have not been performed).
Data on the isolation of ursodeoxycholic acid with breast milk are currently not available. If it is necessary to use ursodeoxycholic acid during lactation, the question of stopping breastfeeding should be solved.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in liver failure.
SPECIAL INSTRUCTIONS
When applying the drug for the purpose of dissolution of gallstones, the following conditions must be observed: the stones must be cholesterol (X-ray negative), their size should not exceed 15-20 mm, the gallbladder should remain functional and should be filled with stones no more than half, the permeability of the cystic and of the common bile duct should be preserved.
For prolonged (more than 1 month) intake of the drug every 4 weeks in the first 3 months of treatment, then a biochemical blood test should be performed every 3 months to determine the activity of hepatic transaminases. Control of the effectiveness of treatment should be carried out every 6 months according to ultrasound of bile ducts.
After complete dissolution of the stones, it is recommended that the use of Ursosan be continued for at least 3 months in order to facilitate the dissolution of stone residues, the sizes of which are too small for their detection and for preventing the recurrence of stone formation.
In experimental studies on animals, mutagenic and carcinogenic effects of ursodeoxycholic acid were not detected.
OVERDOSE
Cases of overdose with ursodeoxycholic acid are not known.
DRUG INTERACTION
When combined, antacids containing aluminum and ion exchange resins (colestyramine) reduce the absorption of UDCA.
With simultaneous use, lipid-lowering drugs (especially clofibrate), estrogens, neomycin or progestins increase the saturation of bile with cholesterol and can reduce the ability of UDCA to dissolve cholesterol bile calculi.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored in a dry, protected from light and out of reach of children at a temperature of 15 В° to 25 В° C. Shelf life - 4 years.
