Urdoksa - instructions for use, dose, side effects, contraindications

Hepatoprotective agent also has choleretic, cholelitholitic, hypocholesterolemic, hypolipidemic, immunomodulating action. It is built into 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 Ca²⁺-dependent alpha protease and stimulates exocytosis, reduces the concentration of toxic bile acids (chenodeoxycholic, lithocholic, deoxycholic, etc.), whose concentrations in patients with chronic liver diseases are increased.

Competitive reduces the absorption of lipophilic bile acids in the intestine, increases their "Fractional" turnover under enterohepatic circulation cholepoiesis induces, promotes the passage of bile and excretion of toxic bile acids across the gut. 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.

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 (Firstly IgM).

Pharmacokinetics:

Ursodeoxycholic acid (UDCA) is absorbed in the small intestine due to passive diffusion (about 90%), and in the ileum through active transport. The maximum concentration in the blood plasma (C_m_Oh) with ingestion of 50 mg after 30, 60, 90 minutes 0 3.8 mmol / l, 5.5 mmol / l and 3.7 mmol / l, respectively. FROM_m_Oh is achieved in 1-3 hours. The connection with plasma proteins is high - up to 96-99%. Penetrates through the placental barrier. With the systematic administration of the drug UDCA becomes the main bile acid in the 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 UDCA in the bile.

Metabolised in the liver (clearance at the "primary passage" through the liver) into taurine and glycine conjugates. The resulting conjugates are secreted in bile.

About 50-70% of the total dose of the drug is excreted with bile. A small amount of non-sucked UDCA 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 different genesis

■ Biliary dyskinesia

Contraindications:

X-ray positive (with a high content of calcium) gallstones, a dysfunctional gallbladder, acute infectious and inflammatory diseases of the gallbladder, bile ducts and intestines, cirrhosis of the liver in the stage of decompensation, pronounced 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.

Carefully:

Carefully used in children aged 3 to 4 years, as it is difficult to swallow capsules.

Pregnancy and lactation:

In experimental animal studies, mutagenic and carcinogenic effects of UDCA were not detected. The use of UDCA 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 UDCA is necessary in the lactation period, the question of stopping breastfeeding should be addressed. Data on the isolation of ursodeoxycholic acid with breast milk are currently not available.

Dosing and Administration:

Urdox® 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 ± 2 mg ursodeoxycholic acid per 1 kg of body weight). In the first 3 months of treatment, taking Urdox® 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 mass	Daily dose	morning	afternoon	evening
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
Over 110 kg	7 capsules	2	2	about

Urdox® 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 per day, which corresponds to:

Body mass	Daily dose
Up to 60 kg	2 capsules
61-80 kg	3 capsules
81-100 kg	4 capsules
Over 100 kg	5 capsules

Urdox® 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.

Treated biliary reflux gastritis

1 capsule of Urdox® daily 1 times a 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.The 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 from 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 from 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 different genesis

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 UDCA are prescribed individually at a rate of 10-20 mg / kg / day.

Side effects:

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 <0.01%); very rarely (<0.01%).

From the gastrointestinal tract: often - diarrhea; rarely - nausea, vomiting; very rarely - acute pain in the right upper abdomen.

From the liver and bile ducts: rarely - a transient increase in the activity of "hepatic" 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 specified in the instruction are aggravated, or if you notice any other undesirable phenomena not listed in the manual, inform the doctor about it.

Overdose:

Cases of overdose UDCA are not known. In case of an overdose, symptomatic treatment is performed.

Interaction:

Kolestyramine, colestipol and antacids containing aluminum hydroxide or smectite (aluminum oxide), reduce the absorption of UDCA in the intestine and thus reduce its absorption and efficacy. If the use of drugs containing at least one of these substances is still necessary, they should be taken at least 2 hours before taking Urdox®.

Ursodeoxycholic acid can enhance the absorption of cyclosporine from the intestine. Therefore, in patients receiving ciclosporin, the doctor should check the concentration of cyclosporine in the blood and adjust the dose of cyclosporine, if necessary.

In some cases, the drug Urdoksa ® can reduce the absorption of ciprofloxacin. Lipid-lowering drugs (especially clofibrate), estrogens, neomycin or progestins increase bile saturation with cholesterol and may decrease the ability to dissolve cholesterol bile stones.

You should inform your doctor about all the medications that you are taking.

Special instructions:

Urdox® should be taken under medical supervision.

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 prolonged (more than 1 month) drug intake, every 4 weeks in the first 3 months of treatment,in the future - every 3 months you need 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 examination of the biliary tract. After completely dissolving the stones, it is recommended that the drug be continued for at least 3 months in order to facilitate the dissolution of stone remains that are too small to detect and prevent the recurrence of stone formation.

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 dosage (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.

Effect on the ability to drive transp. cf. and fur:

Effects on the ability to drive vehicles and work with mechanisms were not identified.

Form release / dosage:

Capsules 250 mg.

Packaging:

10 capsules per contour cell packaging made of polyvinylchloride film and aluminum foil printed lacquered.

For 50 or 100 capsules in cans of polymeric or polymer cans with lids for medicines. The can lid can be made of yellow plastic.

Each label is labeled with a writing or label paper or a self-adhesive label.

One bank or 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 contour mesh packages together with the instruction for use are placed in a cardboard box.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the expiry date printed on the package.

When eliminating unused packages of the drug, special precautions are not required.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001873/09

Date of registration:13.03.2009 / 16.12.2015

Expiration Date:Unlimited

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp14.07.2016

Illustrated instructions

Instructions

Urdox® (Urdoxa)