Urdoxa capsules 250mg, 100pcs

Composition

Per capsule: Active ingredient:  ursodeoxycholic acid. auxiliary substances:  corn starch-73.0 mg, colloidal anhydrous silicon dioxide-5.0 mg, magnesium stearate-2.0 mg. solid gelatin capsule: gelatin-98%, titanium dioxide (E171) – 2%.

Pharmacological action

Pharmacodynamics

A hepatoprotective agent, it also has choleretic, cholelitolytic, hypocholesterolemic, and immunomodulatory effects. It is embedded in the hepatocyte membrane, stabilizes its structure and protects the hepatocyte from the damaging effect of bile acid salts, thus reducing their cytotoxic effect.

In cholestasis, it activates Ca2+ – dependent alpha-protease and stimulates exocytosis, reduces the concentration of toxic bile acids (chenodeoxycholic, litocholic, deoxycholic, etc. ), the concentrations of which are increased in patients with chronic liver diseases.

Competitively reduces the absorption of lipophilic bile acids in the intestine, increases their “fractional” turnover during enterohepatic circulation, induces choleresis, stimulates the passage of bile and the excretion of toxic bile acids through the intestine. It screens nonpolar bile acids (chenodeoxycholic), thereby forming mixed (non-toxic) micelles.

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 biliary system, stimulates the formation and excretion of bile.

Reduces the lithogenicity of bile, increases the concentration of bile acids in it, causes increased gastric and pancreatic secretion, increases the activity of lipase, 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, interleukin-2 formation, reduces the number of eosinophils, suppresses immunocompetent Ig (primarily IgM).

Pharmacokinetics

Ursodeoxycholic acid (UDCA) is absorbed in the small intestine by passive diffusion (about 90%), and in the ileum by active transport.

The maximum concentration in blood plasma (With max ) when taking 50 mg orally after 30,60,90 minutes is 3.8 mmol/l,5.5 mmol/l and 3.7 mmol / l, respectively. C max is reached in 1-3 hours. The connection with plasma proteins is high – up to 96-99%. Penetrates the placental barrier.

When Urdoxa is taken systematically, UDCA 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 UDCA in the bile.

It is metabolized in the liver (clearance during “primary passage” through the liver) to taurine and glycine conjugates. The resulting conjugates are secreted into the bile. About 50-70% of the total dose of the drug is excreted in the bile.

A small amount of unabsorbed UDCA enters the large intestine, where it is broken down by bacteria (7-dehydroxylation), the resulting litocholic acid is partially absorbed from the colon, but is sulfated in the liver and is quickly excreted as a sulfolitocholylglycine or sulfolitocholyltaurine conjugate.

Indications

• Primary biliary cirrhosis in the absence of signs of decompensation;
• dissolution of small and medium cholesterol stones with a functioning gallbladder;
• biliary reflux gastritis.

Use during pregnancy and lactation

Contraindicated during pregnancy and lactation.

Contraindications

• X-ray positive (with a high calcium content) gallstones;
• non-functioning gallbladder;
• acute inflammatory diseases of the gallbladder, bile ducts and intestines;
• liver cirrhosis in the decompensation stage;
• severe renal, liver, and pancreatic dysfunction;
• hypersensitivity to the components of the drug.

Ursodeoxycholic acid has no age restrictions in its 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, because it may be difficult to swallow capsules.

Side effects

the Frequency of adverse reactions is given in accordance with the following classification: very often (>10%); often (>1% and <10%); uncommon (>0.1% and <1%); rarely (>0.01% and <Is 0.1%); very rare (<0,01%). From the gastrointestinal tract: often-diarrhea; rarely-nausea, vomiting; very rarely-acute pain in the right upper abdomen. From the liver and biliary tract: rarely-transient increase in the activity of “liver” enzymes; very rarely-calcification of gallstones. In the treatment of advanced stages of primary biliary cirrhosis, decompensation of liver cirrhosis is very rare, which disappears after discontinuation of the drug. From the skin: very rarely-urticaria. If any of the adverse events listed in the instructions worsen or any other adverse events occur that are not listed in the instructions, tell your doctor.

Interaction

Concomitant use with drugs that reduce intestinal absorption of bile acids (for example, colestyramine) and with drugs that increase biliary elimination of cholesterol (estrogens, hormonal contraceptives, some lipid-lowering agents) is not recommended.

Concomitant use with potentially hepatotoxic drugs is not recommended.

How to take, course of use and dosage

Inside.

For dissolving cholesterol gallstones

The average daily dose is 250-500 mg (after or during meals), which is 1-2 capsules. The course of treatment is from 4-6 months to 12 months or more. The dose for maintenance therapy is 250 mg once a day.

For biliary reflux gastritis

,250 mg once a day. The course of treatment is determined by the doctor.

Symptomatic treatment of primary biliary cirrhosis

The daily dose depends on body weight and ranges from 2 to 6 capsules (approximately 10 to 15 mg of ursodeoxycholic acid per 1 kg of body weight).

Recommended application mode:

• Body weight 34-50 kg: 2 capsules (daily dose); in the morning – 1; in the afternoon – -; in the evening – 1.
• Body weight 51-65 kg: 3 capsules (daily dose); in the morning – 1; in the afternoon-1; in the evening-1.
• Body weight 66-85 kg: 4 capsules (daily dose); in the morning – 1; in the afternoon – 1; in the evening – 2.
• Body weight 86-110 kg: 5 capsules (daily dose); in the morning-1; in the afternoon-2; in the evening-2.
• Body weight over 110 kg: 6 capsules (daily dose); in the morning-2; in the afternoon-2; in the evening-2.

Overdose

Symptoms: increased side effects.

Treatment: carrying out detoxification measures and prescribing colestyramine (for the formation of chelate complexes with bile acids).

Special instructions

When taking the drug for the purpose of dissolving gallstones, the following conditions must be met: the stones must be cholesterol (X-ray negative), their size should not exceed 15 x 20 mm, the gallbladder should remain functional and should be filled with stones no more than half, the patency of the cystic and common bile duct should be preserved.

When taking the drug for a long time (more than 1 month), every 4 weeks in the first 3 months of treatment, and then every 3 months, it is necessary to conduct a biochemical blood test to determine the activity of hepatic transaminases.

Monitoring of the effectiveness of treatment should be carried out every 6 months according to ultrasound examination of the biliary tract. After the stones are completely dissolved, it is recommended to continue using the drug for at least 3 months, in order to promote the dissolution of stone residues, the size of which is too small for their detection and to prevent the recurrence of stone formation.

In patients with frequent attacks of biliary colic, with infectious diseases, changes in the pancreas or intestinal lesions that may alter intrahepatic circulation of bile acids (intestinal resection or ileostomy, limited ileitis), it is advisable to avoid the use of the drug.

Form of production

Capsules

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

4 years

Active ingredient

Ursodeoxycholic acid

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Purpose

For adults as directed by your doctor

Indications

Cholelithiasis, Cirrhosis of the liver