Urdoxa, 250 mg capsules 100 pcs

Pharmacological action
Pharmacological action – hepatoprotective, choleretic, cholelitholytic.

ATH Code
A05A02

Pharmacodynamics

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

It integrates into hepatocyte membrane, stabilizes its structure and protects it from the damaging action of bile acids salts thus reducing their cytotoxic effect. In case of 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 increased in patients with chronic liver diseases.

Concurrently decreases 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.

It shields non-polar bile acids (chenodeoxycholic acid), thus forming mixed (non-toxic) micelles.

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

Increases the solubility of Chs in the biliary system, stimulates the formation and excretion of bile. It decreases lithogenicity of bile, increases concentration of bile acids in it, enhances gastric and pancreatic secretion, increases lipase activity and has hypoglycemic effect.

Causes partial or complete dissolution of cholesterol gallstones, decreases bile Chs saturation that promotes its mobilization from gallstones.

It has immunomodulatory effect, affects immunological reactions in the liver: it decreases the expression of some histocompatibility antigens – HLA-1 on membrane of hepatocytes 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 drug 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.

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 is cleaved by bacteria (7-dehydroxylation); the resulting lithocholic acid is partially absorbed from the colon, but sulfated in the liver and rapidly excreted as sulfolithocholylglycine or sulfolithocholyltaurine conjugate.

Indications

Active ingredient

Composition

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 caps. – 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

The drug Urdoxa® should be taken regularly. The duration of therapy is indefinite.

Dissolution of cholesterol gallstones

The recommended dose is 10 mg UDCA per 1 kg/day (see Table 2).

Table 2

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

The use of the drug Urdox® should be under the supervision of a physician.

When using the drug for dissolution of gallstones the following conditions must be observed: the stones must be cholesterol (X-ray negative), their size must not exceed 15-20 mm, the gallbladder must remain functional and be filled by no more than half, patency of gallbladder and common bile duct must be preserved. At long-term (more than 1 month) administration of the drug every 4 weeks during the first 3 months of treatment, later – every 3 months it is necessary to perform biochemical blood tests to determine the activity of liver transaminases. Control of treatment efficacy should be performed every 6 months by ultrasound of biliary tract. After full dissolution of stones it is recommended to continue the drug use for at least 3 months in order to facilitate dissolution of the remaining stones too small to be detected and for prevention of stone formation recurrence.

In patients with primary biliary cirrhosis, in rare cases, clinical symptoms may worsen at the start of treatment, e.g., pruritus may increase. If this is the case, treatment should be continued with 1 capful daily, then the dosage should be increased (increasing daily dosage by 1 capful weekly) until the recommended dosage regimen is reached again.

If patients have any adverse or serious reactions, they should tell their physician right away, and under no circumstances should they continue to use the drug without their doctor’s recommendation.

No special precautions are required when disposing of unused packages of the drug.

Impact on driving and operating machinery.

There have been no effects on driving and operating machinery.

Contraindications

Side effects

Overdose

If overdose of UDCA is unknown.

Treatment: symptomatic.

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