Urdoxa, capsules 250 mg 50 pcs

Pharmacological action – hepatoprotective, choleretic, cholelitholytic.

Pharmacodynamics

Hepatoprotective drug, also has choleretic, cholestolytic, hypocholesterolemic, hypolipidemic, immunomodulatory action.

It integrates into the membrane of the hepatocyte, stabilizes its structure and protects the hepatocyte from the damaging effects of bile acids salts, thus reducing their cytotoxic effect. In cholestasis it activates Ca2+-dependent α-protease and stimulates exocytosis, decreases concentration of toxic bile acids (chenodeoxycholic acid, lithocholic acid, deoxycholic acid) which concentrations are elevated in patients with chronic liver diseases.

Competitively reduces absorption of lipophilic bile acids in the intestine, increases their fractional turnover in enterohepatic circulation, induces choleresis, stimulates bile passage and excretion of toxic bile acids through the intestine.

Escreens non-polar bile acids (chenodeoxycholic acid), due to which mixed (non-toxic) micelles are formed.

Limits the saturation of bile with Chs by reducing the synthesis and secretion of Chs in the liver and inhibiting its absorption in the intestine.

Enhances the solubility of Chs 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 lipase activity, and has hypoglycemic effect.

Causes partial or complete dissolution of cholesterol gallstones, reduces the saturation of bile with Chs, which promotes its mobilization from gallstones.

It has immunomodulatory effect, influences immunological reactions in the liver: it decreases the expression of some histocompatibility antigens – HLA-1 on hepatocyte membrane and HLA-2 on cholangiocytes, affects the number of T-lymphocytes, IL-2 formation, decreases the number of eosinophils, suppresses immunocompetent Ig (primarily IgM).

Pharmacokinetics

UDCA is absorbed in the small intestine by passive diffusion (about 90%) and in the ileum by active transport. Cmax in plasma when administered orally at a dose of 50 mg after 30, 60, 90 min is 3.8, 5.5 and 3.7 mmol/l, respectively. Cmax is reached after 1-3 hours.

The binding to plasma proteins is high – up to 96-99%. It penetrates through the placental barrier. If UDCA takes the preparation systematically, it becomes the main bile acid in blood serum and forms about 48% of total amount of bile acids in blood. The therapeutic effect of the drug depends on the concentration of UDCA in bile.

It is metabolized in the liver (clearance during the first passage through the liver) into taurine and glycine conjugates. The resulting conjugates are secreted into the bile.

About 50-70% of the total dose of the drug is excreted with bile. A small amount of unabsorbed UDCA enters the colon, 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 rapidly excreted as sulfolithocholylglycine or sulfolithocholyltaurine conjugate.

Indications

Active ingredient

Composition

In one capsule:

active ingredient:
ursodeoxycholic acid.

auxiliary substances:
corn starch – 73.0 mg,
colloidal anhydrous silica – 5.0 mg,
magnesium stearate – 2.0 mg.
Solid gelatin capsule: gelatin – 98%, titanium dioxide (E171) – 2%.

How to take, the dosage

Ingestion, without chewing, with a small amount of water.

Symptomatic treatment of primary biliary cirrhosis

The daily dose depends on body weight and is 3 to 7 capsules. – approximately (14±2) mg UDCA per 1 kg. In the first 3 months of treatment, the dose of the drug Urdox® should be divided into several doses during the day. After improvement of hepatic parameters the daily dose of the drug can be taken once, in the evening.

The following regimen is recommended (see Table 1).

Table 1

Interaction

Colestyramine, colestipol and antacids containing aluminum hydroxide or smectite (aluminum oxide) reduce 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 necessary, they should be taken at least 2 h before taking Urdox®.

UDCA may enhance the absorption of cyclosporine from the intestine. Therefore, in patients taking cyclosporine, the blood concentration of cyclosporine should be checked and the dose of cyclosporine should be adjusted if necessary.

In individual cases the drug Urdoxa® may decrease absorption of ciprofloxacin.

Hypolipidemic drugs (especially clofibrate), estrogens, neomycin or progestins increase bile cholesterol saturation and may decrease the ability to dissolve cholesterol-laden gallstones.

You should tell your doctor about any medications you are taking.

Special Instructions

Contraindications

Overdose

Pregnancy use

The experimental studies on animals did not reveal mutagenic and carcinogenic effects of UDCA. The use of UDCA during pregnancy is possible only when the expected benefits to the mother exceed the potential risk to the fetus (adequate strictly controlled studies on the use of UDCA in pregnant women have not been conducted).

If it is necessary to use the drug during lactation, discontinuation of breastfeeding should be considered. There are currently no data on excretion of UDCA with breast milk.

Similarities