Ursokhol

General characteristics. Structure:

Active ingredient: ursodeoxycholic acid; 1 capsule contains ursodezoksikholevy acid (in terms of 100% dry matter) 250 mg;

excipients: potato starch, methyl cellulose, silicon dioxide colloid anhydrous, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Renders membrane stabilizing, hepatoprotective, cholagogue, holelitichesky and immunomodulatory action. It is built in a hepatocyte membrane, stabilizes its structure and protects a hepatic cell from the striking factors. Competitively inhibits absorption of lipophilic bile acids in intestines, raises their "fractional" turn at enterogepatichesky circulation. Induces bilification, rich with bicarbonates that leads to increase in its passage and stimulates removal of toxic bile acids with a stake. Replacing unpolar bile acids, creates the non-toxic mixed micelles. Slows down synthesis of cholesterol in a liver. Forms rare crystals with cholesterol molecules and interferes with its absorption in intestines, reduces a bile litogennost, reduces a holato-cholesteric index, renders assistance to dissolution of cholesteric stones and prevents their education. At a cholestasia activates Sa2+-zavisimuyu α-proteinase and stimulates an exocytosis, reduces concentration of bile acids (cholic, lithocholic, deoxycholic, etc.).

Immunological activity is caused by reduction of an expression of histocompatibility antigens of HLA-1 on hepatocytes and HLA-2 on holangiotsita, reduces "attack" of immunocompetent immunoglobulins (first of all, Ig M), reduces formation of cytotoxic T lymphocytes.

Pharmacokinetics. After intake of Ursokhol® it is well soaked up in a small bowel due to passive diffusion, and in an ileal gut – by means of active transport. The maximum concentration in plasma is reached within 30 - 60 min. after reception.

At regular use becomes the main bile acid in a blood plasma, making about 96 - 99% of their general contents.

 The maximum concentration in bile is noted at a daily dose 10 - 14 mg/kg. At further increase in a dose concentration of ursodezoksikholevy acid in bile does not increase. Gets through a placental barrier. About 50 - 70% of a dose are removed with bile and partially – with excrements.

Pharmaceutical characteristics.

Main physical and chemical properties: the white, opaque, solid gelatin capsules containing white powder or granules.

Indications to use:

For dissolution of X-ray contrast cholesteric gallstones it is no more than 15 mm in the diameter at patients with the functioning gall bladder, despite presence at it of a bilious stone (it).

For treatment of gastritis with a bile reflux.

For a symptomatic treatment of primary biliary cirrhosis under conditions of absence of dekompensirovanny cirrhosis.

Route of administration and doses:

Apply inside to patients with body weight more than 35 kg.

At different indications the following daily doses are recommended.

For dissolution of cholesteric gallstones.

About 10 mg on 1 kg of body weight a day that answers:

35 - 60 kg           2 capsules
61 - 80 kg            3 capsules
81 - 100 kg           4 capsules
it is more than 100 kg     of 5 capsules

It is necessary to swallow of capsules whole 1 once a day, washing down with a small amount of liquid, in the evening before going to bed.

Capsules need to be used regularly.

Time necessary for dissolution of gallstones, usually makes 6 - 24 months. If reduction of the sizes of gallstones is not observed after 12 months, therapy by drug needs to be stopped.

Efficiency of treatment needs to be checked by means of ultrasonography or the cholecystography every 6 months. It is necessary to conduct additional researches for identification of possible calcification of stones. If it happened, treatment needs to be stopped.

 

For treatment of gastritis with a bile reflux.

To accept 1 capsule a day, washing down it with a small amount of liquid, in the evening before going to bed.

The Ursokhol® capsules need usually to be accepted within 10 - 14 days. As a rule, duration of use depends on the course of a disease. Duration of treatment is determined by the doctor individually.

 

For a symptomatic treatment of primary biliary cirrhosis

The daily dose depends on body weight and makes from about 2 to 6 capsules (about 10-15 mg of ursodezoksikholevy acid on 1 kg of body weight). Such scheme of administration of drug is recommended:

 
Body weight              the Daily dose                 Put Morning       Evening
From 35 to 50 kg             2            capsules 1                -              1
From 51 to 65 kg             3                                           capsules 1 1 1
From 66 to 85 kg             4                                          capsules 1 1 2        
From 86 to 110 kg           of 5                                             capsules 1 2 2        
It is more than 110 kg             of 6                                             capsules 2 2 2                    

It is necessary to swallow of capsules whole, washing down with a small amount of liquid. It is necessary to pay attention to a regularity of reception of capsules.

Use of the Ursokhol® capsules at primary biliary cirrhosis can unlimited time lasts.

In isolated cases at patients with primary biliary cirrhosis in an initiation of treatment clinical symptoms can worsen, for example, the itch can amplify. If it happened, therapy needs to be continued using 1 Ursokhol® capsule a day, and then gradually to increase a dose (by 1 capsule every week) before achievement of the recommended dose.

Features of use:

Use during pregnancy or feeding by a breast. Drug is contraindicated during pregnancy and feeding by a breast. Women of childbearing age can accept drug only on condition of use of reliable contraceptives.

Before an initiation of treatment pregnancy has to be excluded.

Children. Drug is contraindicated to children with body weight to 35 kg.

The Ursokhol® capsules should be used under observation of the doctor.

Efficiency of treatment needs to be checked by means of ultrasonography or the cholecystography every 6 months. It is necessary to conduct additional researches for identification of possible calcification of stones. If it happened, treatment should be stopped.

For the first 3 months of treatment it is necessary to check parameters of function of a liver (nuclear heating plant (SGOT) aspartate aminotransferase, ALT (SGPT) alaninetransaminase and g-GT gamma глутамилтранспептидаза) every 4 week, and then – every 3 month.

Ability to influence speed of response at control of motor transport or work with other mechanisms. Does not influence.

Side effects:

Side effects from digestive tract: liquid excrements or diarrhea during therapy by ursodezoksikholevy acid (often).

At treatment of primary biliary cirrhosis display of pain in the right upper part of an abdominal cavity is possible (very seldom).

Disturbances from gepatobiliarny system (very seldom): at treatment calcification of gallstones can be observed by ursodezoksikholevy acid.

At therapy of the developed stages of primary biliary cirrhosis the decompensation of hepatic cirrhosis which partially regressed after the treatment termination was observed.

Reactions of hypersensitivity it is (very rare): rash can be observed.

Interaction with other medicines:

The УрсохолÒ capsules cannot be used along with Colestyraminum, kolestipoly or the antiacid drugs containing aluminum hydroxide and (or) smectite (aluminum oxide) as these drugs connect ursodezoksikholevy acid in intestines and thus reduce its absorption and efficiency. If use of the drugs containing one of these substances nevertheless is necessary, they need to be applied at least for 2 h to or after reception of the УрсохолÒ capsules.

In some cases the УрсохолÒ capsules can reduce ciprofloxacin absorption.

Урсохол® can strengthen absorption of cyclosporine from intestines. Therefore, at the patients applying cyclosporine it is necessary to check concentration of cyclosporine in blood and in case of need to modify a cyclosporine dose.

Increases effect of peroral antidiabetic means.

Ursodezoksikholevy acid reduces the maximum concentration in plasma and the area under a curve of the calcic antagonist of a nitrendipin. Proceeding from it, and also from one message on interaction with substance dapsone (reduction of therapeutic effect) and from the researches in vitro, it is possible to assume that ursodezoksikholevy acid induces activity of the P450 3A4 cytochrome metabolizing drug.

Therefore at simultaneous use of the means which are metabolized with the participation of this enzyme it is necessary to be careful and consider possibility of need for dose adjustment.

Contraindications:

Hypersensitivity to drug components.

Patients with a gall bladder which is not visualized by radiological methods, calcific stones of a gall bladder, the broken contractility of a gall bladder, patients with frequent bilious gripes.

Acute inflammation of a gall bladder or biliary tract; impassability of bilious channels.

Cirrhosis in a decompensation stage.

Body weight is up to 35 kg (for this form of drug).

Pregnancy and period of feeding by a breast.

Overdose:

Symptoms: at overdose diarrhea is possible.

Treatment: drug phase-out. A symptomatic treatment with preservation of balance of liquid and electrolytes.

Storage conditions:

Period of validity. 2 years. To store in the place, unavailable to children, in original packaging at a temperature from 15 °C to 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 capsules in a blister strip packaging, on 5 or 10 blister strip packagings in a pack.