Ursosan Forte, 500 mg 50 pcs

Hepatoprotective drug. It also has choleretic, cholitholytic, hypolipidemic, hypocholesterolemic and immunomodulatory effects. Having high polar properties, ursodeoxycholic acid (UDCA) is embedded in the membrane of hepatocyte, cholangiocyte and gastrointestinal epithelial cell, stabilizes its structure and protects the cell from the damaging effects of salts of toxic bile acids, thus reducing their cytotoxic effect.

It forms non-toxic mixed micelles with lipophilic (toxic) bile acids, which reduces the ability of gastric refluxate 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, lithocholic, deoxycholic, etc.), whose concentrations are elevated in patients with chronic liver disease. By reducing their concentrations and stimulating bicarbonate-rich choleresis, UDCA effectively contributes to the resolution of intrahepatic cholestasis. Competitively reduces absorption of lipophilic bile acids in the intestine, increases their “fractional” turnover in enterohepatic circulation, induces choleresis, stimulates the passage of bile and excretion of toxic bile acids through the intestine.

Limits bile saturation with cholesterol due to inhibition of its absorption in intestine, suppression of its synthesis in liver and decrease of secretion into bile; promotes gradual disintegration of cholesterol gallstones, which is achieved mainly due to dispersion of cholesterol and formation of liquid crystals; reduces lithogenic index of bile, increases concentration of bile acids in it. The result is the dissolution of cholesterol gallstones and prevention of formation of new concrements.

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

Immunomodulatory action of UDCA is caused by inhibition of expression of histocompatibility antigens – HLA-1 – on membranes of hepatocytes and HLA-2 – on cholangiocytes; normalization of natural killer activity of lymphocytes, formation of interleukin-2, decrease of eosinophils quantity, suppression of immunocompetent immunoglobulins (Ig), primarily IgM regulation of apoptosis of hepatocytes and epitheliocytes of gastrointestinal tract. Delays the progression of fibrosis.

Indications

Hepatitis, Biliary colic, Biliary dyskinesia, Liver cirrhosis, Colic, Pain, Liver damage, Alcoholism, Reflux esophagitis, Gallstone disease, Constipation

– Uncomplicated gallstone disease: Biliary sludge; dissolution of cholesterol gallstones in a functioning gallbladder; prevention of recurrence of stone formation after cholecystectomy;

– Chronic hepatitis of various genesis (including.ч.

– cholestatic liver diseases of various genesis, including primary biliary cirrhosis (with no decompensation symptoms), primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis);

– nonalcoholic fatty liver disease, includingч. non-alcoholic steatohepatitis;

– alcoholic liver disease;

– chronic viral hepatitis;

– biliary dyskinesia;

– biliary reflux gastritis and reflux esophagitis.

Active ingredient

Ursodeoxycholic acid

Composition

1 tablet – ursodeoxycholic acid 500 mg

Associated 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.

Shell contents:

Opadray white 03B28796 – 5 mg (hypromellose 6 – 3.13 mg, titanium dioxide – 1.56 mg, macrogol 400 – 0.31 mg).

How to take, the dosage

It is taken orally, during or after meals, without chewing, with plenty of water.

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

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 the gallstones do not become smaller after 12 months of treatment, the drug should be discontinued.

In order to prevent recurrent stone formation, it is recommended to use the drug for several months after the stones have dissolved.

To prevent recurrence of cholelithiasis after cholecystectomy, 250 mg (1 capsule or 1/2 tablet) 2 times daily for several months.

In chronic hepatitis of different genesis (including toxic, medicinal), chronic viral hepatitis, nonalcoholic fatty liver disease, including nonalcoholic steatohepatitis, alcoholic liver disease average daily dose is 10-15 mg/kg in 2-3 course. The therapy duration is 6-12 months or more.

In cholestatic liver diseases of various genesis, including primary biliary cirrhosis (without decompensation symptoms), primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis) an 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 of biochemical blood parameters, the daily dose of the drug is taken once at night. The therapy duration is from 6 months to several years.

In biliary dyskinesia the average daily dose is 10 mg/kg in 2 doses for 2 weeks to 2 months. If necessary, it is recommended to repeat the treatment course.

In biliary reflux gastritis and reflux esophagitis the average daily dose is 250 mg (1 capful or 1/2 tablet) once at 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

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Interaction

The drug should not be used simultaneously with antacids containing aluminum, ion exchange resins (colestyramine, colestipol), because these drugs may reduce absorption of ursodeoxycholic acid. If necessary, these drugs should be taken 2 hours before or 2 hours after taking UDCA.

Some medications, such as estrogens, progestogens (oral contraceptives), neomycin, and clofibrate, may increase cholithiasis, thereby having the opposite effect to the ability of ursodeoxycholic acid to dissolve cholesterol-laden gallstones.

Ursodeoxycholic acid may increase absorption of cyclosporine from the intestine, which requires monitoring of plasma cyclosporine concentrations and, if necessary, adjustment of its dosing regimen.

In individual cases ursodeoxycholic acid may decrease absorption of ciprofloxacin.

Special Instructions

The drug application for dissolution of gallstones is possible under the following conditions: cholesterol stones (X-ray negative), their size – not more than 15-20 mm, a functioning gallbladder with preserved patency of gallbladder and common bile duct, filled with gallstones not more than by half.

After complete dissolution of the stones it is recommended to continue treatment for 3 months in order to facilitate dissolution of the remaining stones too small to be detected and to prevent stone recurrence.

Impact on ability to drive vehicles and mechanisms

The use of Ursosan does not affect potentially hazardous activities requiring increased concentration and quick psychomotor reactions (including the ability to drive vehicles and operate moving mechanisms).

Contraindications

– hypersensitivity to the active and excipient components of the drug;

– X-ray-positive (high calcium content) gallstones;

– non-functioning gallbladder;

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

– decompensated cirrhosis of the liver;

– Severe renal dysfunction;

– Severe liver dysfunction;

– Severe pancreatic dysfunction.

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

Side effects

Definition of the frequency of adverse effects (number of cases/number of observations): very common (≥1/10); common (≥1/100 to < 1/10); infrequent (≥1/1000 to < 1/100); rare (≥1/10 000 to < 1/1000); very rare (< 1/10 000), frequency cannot be calculated from available data.

Digestive system disorders: in clinical trials diarrhea or pasty stools were frequently observed during treatment with ursodeoxycholic acid. Severe upper abdominal pain was very rarely observed during treatment of primary biliary cirrhosis.

Liver and biliary tract disorders: Calcification of gallstones was observed in very rare cases during treatment with ursodeoxycholic acid.

When treating primary biliary cirrhosis at late stages, decompensation of liver cirrhosis was observed in very rare cases, which regressed after discontinuation of treatment.

Skin and subcutaneous tissues: in very rare cases urticaria may be observed.

Overdose

Symptoms: diarrhea may occur in case of overdose.

Other symptoms of overdose are unlikely because resorption of ursodeoxycholic acid worsens as the dose increases, leading to increased excretion in the feces.

Treatment: In case of persistent diarrhea the drug therapy should be discontinued. Treatment is symptomatic.

Pregnancy use

The use of ursodeoxycholic acid in pregnancy is possible only when the expected benefits to the mother exceed the potential risk to the fetus or the newborn (adequate strictly controlled trials of ursodeoxycholic acid in pregnant women have not been conducted).

Similarities

Ursofalk, Urdoxa, Ursoliv, Exchol, Ursodez, Grinterol, Urcevel, Ursodeoxycholic acid