Composition, form of production and packaging
Capsules hard gelatinous, size No. 0, white or almost white, opaque; the content of the capsules is a white or almost white powder or granulate.
1 caps.
ursodeoxycholic acid 250 mg
Excipients: corn starch - 73 mg, silicon dioxide colloidal anhydrous - 5 mg, magnesium stearate - 2 mg.
The composition of the capsule is hard gelatinous: gelatin - 98%, titanium dioxide (E171) - 2%.
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (4) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
10 pieces. - packings cellular planimetric (6) - packs cardboard.
10 pieces. - packings cellular planimetric (7) - packs cardboard.
10 pieces. - packings cellular planimetric (8) - packs cardboard.
10 pieces. - packings cellular planimetric (9) - packs cardboard.
10 pieces. - packings cellular planimetric (10) - packs cardboard.
50 pcs. - polymer cans (1) - packs of cardboard.
100 pieces. - polymer cans (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
Hepatoprotective agent, has choleretic, cholelitholitic, hypocholesterolemic, hypolipidemic, immunomodulating action.
It is embedded in the membrane of the hepatocyte, stabilizes its structure and protects the hepatocyte from damaging effects of bile salts, thus reducing their cytotoxic effect. When cholestasis activates Ca 2+ -dependent alpha protease and stimulates exocytosis, reduces the concentration of toxic bile acids (chenodeoxycholic, lithocholic, deoxycholic and others), whose concentrations in patients with chronic liver diseases are increased.
Competitively reduces the absorption of lipophilic bile acids in the intestine, increases their "fractional" turnover with enterohepatic circulation, induces choleresis, stimulates bile passage and the excretion of toxic bile acids through the intestine.
It screens nonpolar bile acids (chenodeoxycholic), due to which mixed (non-toxic) micelles are formed.
Reduces the saturation of bile with cholesterol by reducing the synthesis and secretion of cholesterol in the liver and inhibiting its absorption in the intestine.
Increases the solubility of cholesterol in the bile excretory system, stimulates the formation and secretion of bile. It reduces the lithogenicity of bile, increases the concentration of bile acids in it, causes an increase in gastric and pancreatic secretion, increases lipase activity, and has a hypoglycemic effect.
Causes partial or complete dissolution of cholesterol gallstones, reduces the saturation of bile with cholesterol, which contributes to its mobilization from gallstones.
It has an immunomodulatory effect, affects immunological reactions in the liver: reduces the expression of certain histocompatibility antigens - HLA-1 on the membrane of hepatocytes and HLA-2 on cholangiocytes, affects the number of T-lymphocytes, the formation of interleukin 2, reduces the number of eosinophils, suppresses immunocompetent Ig (in first of all IgM).
PHARMACOKINETICS
Suction
Ursodeoxycholic acid is absorbed in the small intestine due to passive diffusion (about 90%), and in the ileum through active transport. C max when ingested at a dose of 50 mg after 30, 60, 90 minutes - 3.8 mmol / l, 5.5 mmol / l and 3.7 mmol / l, respectively, and is achieved in 1-3 hours.
Distribution
Binding to plasma proteins is high - up to 96-99%. Penetrates through the placental barrier. With the systematic administration of the drug 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 the bile.
Metabolism and excretion
Metabolised in the liver (clearance at the "first 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 unsweetened 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
- primary biliary cirrhosis in the absence of signs of decompensation (symptomatic treatment);
- dissolution of gallstones cholesterol stones;
- Biliary reflux-gastritis;
- primary sclerosing cholangitis;
- alcoholic liver disease;
- non-alcoholic steatohepatitis;
- Cystic fibrosis (cystic fibrosis);
- chronic hepatitis of various genesis;
- biliary dyskinesia.
DOSING MODE
Urdox В® capsules are taken orally, without chewing, with a small amount of water.
Symptomatic treatment of primary biliary cirrhosis
The daily dose depends on the body weight and is from 3 to 7 capsules (about 14 В± 2 mg ursodeoxycholic acid per 1 kg of body weight). In the first 3 months of treatment, taking Urdox В® should be divided into several doses during the day. After improving liver function, the daily dose of the drug can be taken 1 time, in the evening.
The following application mode is recommended:
Body weight Daily dose in the morning in the afternoon
34-46 kg 2 capsules 1 - 1
47-62 kg 3 capsules 1 1 1
63-78 kg 4 capsules 1 1 2
79-93 kg 5 capsules 1 2 2
94-109 kg 6 capsules 2 2 2
More than 110 kg 7 capsules 2 2 3
Urdox В® should be taken regularly. Duration of therapy - for unlimited time.
Dissolution of gallstones cholesterol stones
The recommended dose is 10 mg ursodeoxycholic acid per 1 kg of body weight / day, which corresponds to:
Body weight Daily dose
Up to 60 kg 2 capsules
61-80 kg 3 capsules
81-100 kg 4 capsules
Over 100 kg 5 capsules
Urdox В® should be taken every evening, before bedtime. The duration of therapy is 6-12 months. For the prevention of repeated cholelithiasis, the use of the drug is recommended for several months after the dissolution of the stones.
Treatment of biliary reflux gastritis
1 capsule of the drug Urdoks В® daily 1 time / day before bedtime. The course of treatment is from 10-14 days to 6 months, if necessary up to 2 years.
Primary sclerosing cholangitis
The daily dose is 12-15 mg / kg; if necessary, the dose may be increased to 20-30 mg / kg in 2-3 doses. Duration of therapy is from 6 months to several years.
Alcoholic liver disease
The average daily dose is 10-15 mg / kg in 2-3 doses. The duration of therapy is 6-12 months or more.
Non-alcoholic steatohepatitis
The average daily dose is 10-15 mg / kg in 2-3 doses. The duration of therapy is 6-12 months or more.
Cystic fibrosis (cystic fibrosis)
The daily dose is 12-15 mg / kg; if necessary, the dose may be increased to 20-30 mg / kg in 2-3 doses. Duration of therapy is from 6 months to several years or for life.
Chronic hepatitis of various origins
The daily dose is 10-15 mg / kg in 2-3 divided doses. The duration of therapy is 6-12 months or more.
Biliary dyskinesia
The average daily dose is 10 mg / kg in 2 divided doses. The duration of therapy is from 2 weeks to 2 months. If necessary, the course of treatment is recommended to be repeated.
Children over 3 years of age, the drug is administered individually at a rate of 10-20 mg / kg / day.
SIDE EFFECT
The frequency of unwanted reactions is given in accordance with the following scale: very often (> 10%); often (> 1% and <10%); infrequently (> 0.1% and <1%);rarely (> 0.01% and <0.1%); very rarely (<0.01%).
From the gastrointestinal tract: often - diarrhea; rarely - nausea, vomiting, transient increase in the activity of liver enzymes; very rarely - calcification of gallstones. In the treatment of advanced stages of primary biliary cirrhosis is very rare - decompensation of liver cirrhosis, which disappears after drug withdrawal.
From the skin: very rarely - hives.
If any of the undesirable effects indicated in the instruction are aggravated or any other undesirable phenomena not indicated in the instruction appear, inform the doctor about it.
CONTRAINDICATIONS
- X-ray positive (high in calcium) gallstones;
- non-functioning gallbladder;
- acute inflammatory diseases of the gallbladder, bile ducts and intestines;
- cirrhosis of the liver in the stage of decompensation;
- marked violations of the kidneys, liver, pancreas;
- Hypersensitivity to the components of the drug.
Ursodeoxycholic acid has no age limitation in use, but children under 3 years of age are not recommended to use the drug in this dosage form.
Use with caution in children aged 3 to 4 years, t. possible difficulty in swallowing capsules.
PREGNANCY AND LACTATION
In experimental studies on animals, mutagenic and carcinogenic effects of ursodeoxycholic acid have not been revealed. The use of the drug 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).
If you need to use the drug during lactation, you should decide whether to stop breastfeeding. Data on the isolation of ursodeoxycholic acid with breast milk are currently not available.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindication: severe renal dysfunction.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindication: marked violations of liver function, cirrhosis of the liver in the stage of decompensation.
APPLICATION FOR CHILDREN
Ursodeoxycholic acid has no age limitation in use, but children under 3 years of age are not recommended to use the drug in this dosage form.
Use with caution in children aged 3 to 4 years, t. possible difficulty in swallowing capsules.
Children over 3 years of ursodeoxycholic acid are prescribed individually at a rate of 10-20 mg / kg / day.
SPECIAL INSTRUCTIONS
Taking Urdox В® should be done under the supervision of a doctor.
When taking the drug for the purpose of dissolution of gallstones, it is necessary to observe the following conditions: 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. With long-term (more than 1 month) drug intake every 4 weeks in the first 3 months of treatment, further - every 3 months it is necessary to conduct a biochemical blood test 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 completely dissolving the stones, it is recommended to continue the use of the preparation for at least 3 months in order to facilitate the dissolution of stone remains, the sizes of which are too small for their detection and for the prevention of stone recurrence.
In patients with primary biliary cirrhosis, in rare cases, clinical symptoms may worsen at the beginning of treatment, for example, itching may increase. In this case, the treatment should continue, taking 1 capsule daily, then you should increase the dose (increasing the daily dose weekly by 1 capsule) until the recommended dosage regimen is again achieved.
In case of unwanted or severe reactions, the patient should immediately inform the attending physician about them and, in no case, continue taking the drug without his recommendation.
Impact on the ability to drive vehicles and manage mechanisms
Effects on the ability to drive vehicles and work with mechanisms were not identified.
OVERDOSE
Cases of overdose of ursodeoxycholic acid are unknown. In case of an overdose, symptomatic treatment is recommended.
DRUG INTERACTION
Colestramine, colestipol and antacids containing aluminum hydroxide or smectite (aluminum oxide), reduce the absorption of ursodeoxycholic acid in the intestine and, thus, reduce its absorption and efficiency. If the use of drugs containing at least one of these substances is necessary, they should be taken at least 2 hours before taking Urdox В® .
Ursodeoxycholic acid can increase the absorption of cyclosporine from the intestine. Therefore, in patients taking cyclosporine, you should check the concentration of cyclosporine in the blood and adjust the dose of cyclosporine, if necessary.
In some cases, the drug Urdoksa В® can reduce the absorption of ciprofloxacin.
Lipid-lowering drugs (especially clofibrate), estrogens, neomycin or gestagens increase the saturation of bile with cholesterol and may reduce the ability to dissolve cholesterol bile stones.
The patient should inform the doctor about all the medications he is taking.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 4 years.
Do not use after the expiry date printed on the package.
