Ursosan Forte pills 500mg, 100pcs

Composition

1 tab. – ursodeoxycholic acid 500 mg

Auxiliary substances:

corn starch-94.5 mg,

pregelatinized corn starch-48 mg,

sodium carboxymethyl starch (type A) – 13 mg,

colloidal silicon dioxide-15 mg,

magnesium stearate-14.5 mg

Pharmacological action

Hepatoprotective drug. It also has choleretic, cholelitolytic, hypolipidemic, hypocholesterolemic and immunomodulatory effects. Having high polar properties, ursodeoxycholic acid (UDCA) is embedded in the membrane of the hepatocyte, cholangiocyte and epithelial cell of the gastrointestinal tract, stabilizes its structure and protects the cell from the damaging effect of toxic bile acid salts, thus reducing their cytotoxic effect. It forms non-toxic mixed micelles with lipophilic (toxic) bile acids, which reduces the ability of gastric reflux to damage cell membranes in cholestatic liver diseases, biliary reflux gastritis and reflux esophagitis.

In cholestasis, UDCA activates Ca2-dependent alpha-protease and stimulates exocytosis, reduces the concentration of toxic bile acids (chenodeoxycholic, litocholic, deoxycholic, etc. ), the concentrations of which are elevated in patients with chronic liver diseases. By reducing their concentration and stimulating bicarbonate-rich choleresis, UDCA effectively promotes resolution of intrahepatic cholestasis. 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.

Reduces the saturation of bile with cholesterol by inhibiting its absorption in the intestine, suppressing synthesis in the liver and reducing secretion into the bile; promotes the gradual breakdown of cholesterol gallstones, which is achieved mainly due to the dispersion of cholesterol and the formation of liquid crystals; reduces the litogenic index of bile, increases the concentration of bile acids in it. The result is the dissolution of cholesterol gallstones and the prevention of the formation of new stones.

Causes increased gastric and pancreatic secretion, increases lipase activity, and has a hypoglycemic effect.

The immunomodulatory effect of UDCA is due to inhibition of the expression of histocompatibility antigens – HLA-1-on hepatocyte membranes and HLA-2-on cholangiocytes, normalization of the natural killer activity of lymphocytes, formation of interleukin – 2, a decrease in the number of eosinophils, suppression of immunocompetent immunoglobulins (Ig), primarily IgM; regulation of apoptosis of hepatocytes and gastrointestinal epithelial cells. Delays the progression of fibrosis.

Indications

: uncomplicated gallstone disease: biliary sludge; dissolution of cholesterol gallstones in a functioning gallbladder; prevention of stone recurrence after cholecystectomy;

— chronic hepatitis of various origins (including toxic, medicinal);

— cholestatic liver diseases of various Genesis, including primary biliary cirrhosis (without signs of decompensation), primary sclerosing cholangitis, cystic fibrosis (mucoviscidosis);

— non-alcoholic fatty liver disease, including nonalcoholic steatohepatitis;

alcoholic liver disease;

chronic viral hepatitis;

— dyskinesia of the biliary tract

— the biliary reflux gastritis and reflux esophagitis.

Contraindications

— hypersensitivity to the active and auxiliary components of the drug;

— roentgenologically (high in calcium) gallstones;

— non-functioning gall bladder

— acute inflammatory diseases of the gallbladder, bile ducts and intestines;

liver cirrhosis in the stage of decompensation;

— severe renal dysfunction;

— pronounced violations of the liver;

is expressed by the human pancreas.

Ursodeoxycholic acid has no age restrictions for use, but it is not recommended to use the drug in this dosage form in children under 3 years of age.

Side effects

Determination of the frequency of side effects (number of cases/number of observations): very common (≥1/10); common (≥1/100 to < 1/10); infrequent (≥1/1000 to

From the digestive system:  in clinical studies, diarrhea or pasty stools were frequently observed during ursodeoxycholic acid treatment. In the treatment of primary biliary cirrhosis, severe upper abdominal pain was very rarely observed.

Liver and biliary tract disorders:  Calcification of gallstones was observed in very rare cases during treatment with ursodeoxycholic acid. In the treatment of late-stage primary biliary cirrhosis, decompensation of liver cirrhosis was observed in very rare cases, which regressed after discontinuation of treatment.

Skin and subcutaneous tissue disorders:  in very rare cases, urticaria may occur.

Interaction

Do not use the drug simultaneously with antacids containing aluminum, ion-exchange resins (colestyramine, colestipol), since these drugs can reduce the absorption of ursodeoxycholic acid. If necessary, these medications should be taken 2 hours before or 2 hours after taking UDCA.

Some medications, such as estrogens, progestogens (oral contraceptives), neomycin, clofibrate, can increase cholelithiasis, thereby having the opposite effect of the ability of ursodeoxycholic acid to dissolve cholesterol bile stones.

Ursodeoxycholic acid can increase the absorption of cyclosporine from the intestine, which requires monitoring the concentration of cyclosporine in blood plasma, and, if necessary, correcting its dosage regimen.

In some cases, ursodeoxycholic acid may reduce the absorption of ciprofloxacin.

How to take, course of use and dosage

Take orally, during or after a meal, without chewing, with a sufficient amount of water.

To ensure the recommended dose, the tablet should be divided in half, breaking at risk. Segments that are broken incorrectly should not be used. When the segment is held in the mouth, a bitter taste is felt.

To dissolve cholesterol gallstones, the average daily dose of the drug is 10 mg / kg (up to 12-15 mg / kg). The daily dose of the drug is taken once at night. The course of treatment is 6-12 months or more until the stones are completely dissolved. If gallstones do not decrease in size after 12 months of treatment, the drug should be discontinued.

To prevent the re-formation of stones, it is recommended to use the drug for several months after the dissolution of the stones.

To prevent repeated cholelithiasis after cholecystectomy,250 mg (1 capsule or 1/2 tab. ) is prescribed 2 times a day for several months.

For chronic hepatitis of various origins (including toxic, medicinal), chronic viral hepatitis, non-alcoholic fatty liver disease, including non-alcoholic steatohepatitis, alcoholic liver disease, the average daily dose is 10-15 mg / kg in 2-3 doses. The duration of therapy is 6-12 months or more.

In cholestatic liver diseases of various origins, including primary biliary cirrhosis (in the absence of signs of decompensation), primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis) the average daily dose is 12-15 mg / kg, if necessary-20-30 mg/kg. During the first 3 months of treatment, the daily dose of the drug should be divided into 2-3 doses. In case of improvement in the biochemical parameters of the blood, the daily dose of the drug is taken once a night. The duration of therapy is from 6 months to several years.

For biliary dyskinesia, the average daily dose is 10 mg / kg in 2 divided doses for 2 weeks to 2 months. If necessary, the course of treatment is recommended to be repeated.

For biliary reflux gastritis and reflux esophagitis, the average daily dose is 250 mg (1 capsule or 1/2 tab. ) 1 time per night. The course of treatment is from 2 weeks to 6 months, if necessary-up to 2 years.

Calculation of the daily number of capsules and tablets depending on the patient’s body weight and the recommended dose of the drug per 1 kg of body weight, mg/kg / day

Overdose

Symptoms: in case of overdose, diarrhea may occur. Other symptoms of overdose are unlikely, as ursodeoxycholic acid resorption worsens as the dose increases, leading to increased excretion in the faeces.

Treatment: if prolonged diarrhea persists, therapy with the drug should be discontinued. Treatment is symptomatic.

Special instructions

The use of the drug for the purpose of dissolving gallstones is possible if the following conditions are met: the stones must be cholesterol (X-ray negative), their size-no more than 15-20 mm, a functioning gallbladder with preserved patency of the cystic and common bile duct, filled with gallstones no more than half.

With prolonged use of the drug to dissolve gallstones every 4 weeks in the first 3 months of treatment, in the future-every 3 months, a biochemical blood test should be performed to determine the activity of hepatic transaminases. Monitoring of the effectiveness of treatment should be carried out every 6 months according to ultrasound of the gallbladder, biliary tract.

After the stones are completely dissolved, it is recommended to continue using the drug for 3 months in order to promote the dissolution of stone residues, the size of which is too small for their detection, and in order to prevent the recurrence of stone formation.

Influence on the ability to drive vehicles and mechanisms

The use of Ursosan does not affect the performance of potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions (including the ability to drive vehicles, work with moving mechanisms).

Form of production

Film-coated tablets.

Storage conditions

Tablets should be stored in a place protected from light and at a temperature of 15° to 25°C.

Shelf

life is 3 years.

Active ingredient

Ursodeoxycholic acid

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Children over 3 years of age, Children as prescribed by a doctor, Adults as prescribed by a doctor

Indications

Reflux esophagitis, Liver damage, Cirrhosis of the liver, Biliary dyskinesia, Cholelithiasis, Alcoholism, Hepatitis