Ursosan Forte tablets p / o 500mg, No. 100

• primary biliary cirrhosis in the absence of signs of decompensation (symptomatic treatment);

• dissolution of cholesterol stones of the gallbladder;

• biliary reflux gastritis;

• primary sclerosing cholangitis;

• alcoholic liver disease;

• non-alcoholic steatohepatitis;

• cystic fibrosis (cystic fibrosis);

• chronic hepatitis of various origins;

• biliary dyskinesia.

Inside during or after meals without chewing, drinking plenty of water.

To ensure the recommended dosage, the tablet should be halved, breaking at risk. Broken segments should not be used correctly. When holding the segment in the mouth, a bitter taste is felt.

To dissolve cholesterol gallstones, the average daily dose of the drug is 10 mg / kg of body weight.

During the first 3 months of treatment, the daily dose should be divided into several doses. It usually takes 6-24 months for gallstones to dissolve. If, after 12 months of treatment, the size of the stones does not decrease, then the treatment should be discontinued.

The effectiveness of treatment should be assessed every 6 months by ultrasound or radiography. In the course of an interim examination, it should be assessed whether calculus has occurred over the past period. In case of calcification of stones, treatment should be discontinued.

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

In chronic hepatitis of various origins (toxic medicinal, etc.) 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), the daily dose depends on body weight and ranges from 11/2 to 31/2 tablets (14 ± 2 mg UDCA per 1 kg of body weight). During the first three months of treatment, you should distribute the intake of URSOSANЃFORT tablets throughout the day. If the liver function test values ??improve, the daily dose can be taken once a day in the evening.

The use of the drug URSOSANЃFORTE for the treatment of primary biliary cirrhosis can be continued indefinitely.

In patients with primary biliary cirrhosis, in rare cases, clinical symptoms may worsen at the beginning of treatment, for example, itching may become more frequent. In this case, treatment should be continued by taking 1/2 tablet daily, then the dose should be gradually increased (increasing the daily dose by 1/2 tablet weekly) until the recommended dosage regimen is reached again.

Primary sclerosing cholangitis - daily dose 12-15 mg / kg; if necessary, the dose can be increased to 20 mg / kg in 2-3 divided doses. The duration of therapy is from 6 months to several years (see the section 'Special instructions').

Cystic fibrosis (as part of complex therapy) - the daily dose is 20 mg / kg in 2-3 doses with a further increase to 30 mg / kg if necessary.

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.

With biliary reflux gastritis, the average daily dose is 250 mg (1/2 tablet) once a night. The course of treatment is from 10-14 days to 6 months, if necessary - up to 2 years.

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

1 caps.

active substance: ursodeoxycholic acid - 500 mg

excipients: corn starch - 73 mg; colloidal anhydrous silicon dioxide - 5 mg; magnesium stearate - 2 mg hard gelatin capsule: gelatin - 98%; titanium dioxide (E171) - 2%

• X-ray positive (high calcium) gallstones;

• non-functioning gallbladder;

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

• cirrhosis of the liver in the stage of decompensation;

• severe violations of the kidneys, liver, pancreas;

• hypersensitivity to the components of the drug.

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

Use with caution in children aged 3 to 4 years, because it may be difficult to swallow the capsules.

pharmachologic effect

Hepatoprotective agent, has a choleretic, cholelitholytic, hypocholesterolemic, hypolipidemic, immunomodulatory effect.

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

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.

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

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

Increases the solubility of cholesterol in the biliary system, stimulates the formation and secretion of bile. Reduces the lithogenicity of bile, increases the concentration of bile acids in it, causes an increase in gastric and pancreatic secretion, enhances lipase activity, and has a hypoglycemic effect.

It causes partial or complete dissolution of cholesterol gallstones, reduces the saturation of bile with cholesterol, which contributes to its mobilization from gallstones.

It has an immunomodulatory effect, affects immunological reactions in the liver: reduces the expression of some histocompatibility antigens - HLA-1 on the membrane of hepatocytes and HLA-2 on cholangiocytes, affects the number of T-lymphocytes, the formation of interleukin 2, reduces the number of eosinophils, suppresses immunocompetent Ig (in primarily IgM).

Indications of the drug

• primary biliary cirrhosis in the absence of signs of decompensation (symptomatic treatment);

• dissolution of cholesterol stones of the gallbladder;

• biliary reflux gastritis;

• primary sclerosing cholangitis;

• alcoholic liver disease;

• non-alcoholic steatohepatitis;

• cystic fibrosis (cystic fibrosis);

• chronic hepatitis of various origins;

• biliary dyskinesia.

Dosage regimen

The capsules are taken orally, without chewing, with a little water.

Symptomatic treatment of primary biliary cirrhosis

The daily dose depends on body weight and ranges from 3 to 7 capsules (approximately 14 ± 2 mg ursodeoxycholic acid per 1 kg of body weight). In the first 3 months of treatment, taking the drug UrdoksaЃ should be divided into several doses during the day. After improvement of hepatic parameters, the daily dose of the drug can be taken 1 time, in the evening.

Contraindications for use

• X-ray positive (high calcium) gallstones;

• non-functioning gallbladder;

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

• cirrhosis of the liver in the stage of decompensation;

• severe violations of the kidneys, liver, pancreas;

• hypersensitivity to the components of the drug.

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

Use with caution in children aged 3 to 4 years, because it may be difficult to swallow the capsules.

Side effects:

The frequency of occurrence of side effects (number of cases / number of observations) in accordance with the classification of the World Health Organization is presented in the form of the following gradation: very often (? 1/10); often (? 1/100 to <1/10); infrequently (? 1/1000 to <1/100); rarely (? 1/10000 to <1/1000); very rarely (<1/10 000) the frequency is not set (the frequency cannot be estimated from the available data).

Gastrointestinal disorders:

In clinical studies, diarrhea or loose stools were often observed during treatment with ursodeoxycholic acid.

In the treatment of primary biliary cirrhosis, acute pain in the right upper abdomen was very rare.

Liver and biliary tract disorders:

Calcification of gallstones was observed in very rare cases during treatment with ursodeoxycholic acid.

In the treatment of primary biliary cirrhosis in the late stages, in very rare cases, decompensation of liver cirrhosis was noted, which regressed after discontinuation of the drug.

Skin and subcutaneous tissue disorders:

In very rare cases, allergic reactions, including urticaria, may occur.

If any of the side effects indicated in the instructions are aggravated or you notice other side effects not indicated in the instructions, please inform your doctor.

Overdose:

In case of overdose, diarrhea may occur. With established prolonged diarrhea, drug therapy should be discontinued. Treatment of diarrhea is symptomatic (restoration of water and electrolyte balance).

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

Interaction:

Do not use the drug concurrently with antacids containing aluminum hydroxide or smectite (aluminum oxide) ion exchange resins (cholestyramine colestipol) since these drugs can reduce the absorption of ursodeoxycholic acid in the intestine and thus reduce its absorption and effectiveness. If the use of preparations containing at least one of these substances is nevertheless necessary, they should be taken 2 hours before or 2 hours after taking URSOSANЃFORTE.

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

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

In a clinical study involving healthy volunteers, the simultaneous use of ursodeoxycholic acid (500 mg / day) and rosuvastatin (20 mg / day) led to a slight increase in the level of rosuvastatin in blood plasma. The clinical significance of this interaction, including in relation to other statins, is unknown.

It has been proven that ursodeoxycholic acid reduces the maximum concentration and the area under the pharmacokinetic curve 'concentration-time' of the calcium antagonist nitrendipine. In the case of the simultaneous use of nitrendipine and ursodeoxycholic acid, careful monitoring is recommended. An increase in the dose of nitrendipine may be required. In addition, a decrease in the therapeutic effect of dapsone has been reported.

These data, as well as data obtained in vitro, suggest that ursodeoxycholic acid can induce CYP3A isoenzymes. Nevertheless, the results of controlled clinical trials indicate that ursodeoxycholic acid does not have a pronounced inducing effect on the CYP3A isoenzyme.

Certain medications such as estrogens, progestogens (oral contraceptives) neomycin clofibrate can increase cholelithiasis, thereby countering the effect of ursodeoxycholic acid's ability to dissolve cholesterol gallstones.

Special instructions:

Taking the drug URSOSANЃFORT should be carried out under the supervision of a physician.

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

With long-term use of the drug in order to dissolve gallstones, every 4 weeks in the first 3 months of treatment, and then every 3 months, a biochemical blood test should be performed to determine the activity of microsomal liver enzymes (alkaline phosphatase transaminase and gamma-glutamyl transpeptidase).

Monitoring of these parameters makes it possible to detect abnormal liver function in the early stages. This also applies to patients with advanced stages of primary biliary cirrhosis.

In addition, it can quickly determine whether a patient with primary biliary cirrhosis is responding to the treatment.

When used in patients to dissolve cholesterol gallstones.

In order to assess the progress in treatment and for the timely detection of signs of calcification of stones, depending on the size of the stones, the gallbladder should be visualized (oral cholecystography) with examination of the opacities in the standing and supine position (ultrasound) after 6-10 months after starting treatment.

If the gallbladder cannot be visualized on X-rays or in cases of calcification of stones, weak contractility of the gallbladder or frequent attacks of colic, URSOSANЃFORT should not be used.

When treating patients with advanced stages of primary biliary cirrhosis

Cases of liver cirrhosis decompensation were extremely rare. After discontinuation of therapy, regression of manifestations of decompensation was noted.

In patients with primary biliary cirrhosis, in rare cases, at the beginning of treatment, clinical symptoms may increase, for example, itching may increase. In this case, the dose of the drug must be reduced to 250 mg (1/2 tablet) and then gradually increased again as described in the section 'Dosage and administration'.

Use in patients with primary sclerosing cholangitis

Long-term therapy with high doses of ursodeoxycholic acid (28-30 mg / kg / day) in patients with this pathology can cause serious side effects.

In patients with diarrhea, the dosage should be reduced. If diarrhea persists, treatment should be discontinued.

Women of reproductive age should take URSOSANЃFORTE while using reliable contraception. It is recommended to use non-hormonal contraceptives or low estrogen oral contraceptives because hormonal oral contraceptives can increase gallbladder stones. Possible pregnancy should be excluded before starting treatment.

Impact on the ability to drive vehicles. Wed and fur .:

The use of the drug URSOSANЃFORTENE affects the performance of potentially hazardous activities requiring an increased concentration of attention and speed of psychomotor reactions (the ability to drive vehicles, work with moving mechanisms, etc.).

Release form / dosage:

Film-coated tablets 500 mg.

Packaging:

10 tablets in a blister made of PVC / PVDC / aluminum foil.

1 5 or 10 blister packs (blisters) together with instructions for use are placed in a cardboard box.

Storage conditions:

In a dark place at a temperature of 15 to 25 ? C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date.

Vacation conditions

On prescription

Manufacturer

PRO.MED.CS Prague as, Telcska 1, 140 00 Praha 4, Czech Republic, Czech Republic