Ursodez - SZ capsule 500mg, No. 30

• dissolution of cholesterol stones with a functioning gallbladder;

• primary biliary cirrhosis of the liver in the absence of signs of decompensation;

• chronic hepatitis of various origins;

• primary sclerosing cholangitis;

• cystic fibrosis (cystic fibrosis);

• non-alcoholic steatohepatitis;

• alcoholic liver disease;

• biliary dyskinesia.

The drug is taken orally.

Dissolving cholesterol gallstones

The recommended (approximate) dose is 10 mg of ursodeoxycholic acid per 1 kg of body weight per day. The drug must be taken daily in the evening, before bedtime (the capsules are not chewed), with a small amount of liquid.

It usually takes 6-24 months to dissolve gallstones. 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 recurrent cholelithiasis, it is recommended to take the drug for several months after the stones dissolve.

Symptomatic treatment of primary biliary cirrhosis

The daily dose depends on body weight and ranges from 1 to 3 capsules (500 mg) (approximately 10 to 15 mg ursodeoxycholic acid per 1 kg of body weight) in 2-3 doses, the first 3 months of treatment. After improving the functional parameters of the liver, the daily dose can be applied 1 time in the evening. The duration of the course of treatment is not limited. In rare cases, at the beginning of treatment, clinical symptoms may worsen (itching becomes more frequent). In this case, you should reduce the daily dose (up to 250 mg), and then gradually increase it (weekly increasing the daily dose) until the recommended dosage regimen is reached.

Chronic hepatitis of various origins, non-alcoholic steatohepatitis and alcoholic liver disease

The average daily dose is from 10 to 15 mg of ursodeoxycholic acid per 1 kg of body weight in 2-3 doses. The duration of therapy is 6-12 months or more.

Primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis)

For primary sclerosing cholangitis: 12-15 mg / kg / day (up to 20 mg / kg / day) in 2-3 doses. The duration of use is from 6 months to several years.

With cystic fibrosis (cystic fibrosis): 20-30 mg / kg / day in 2-3 doses. The duration of use is from 6 months to several years.

Biliary dyskinesia

The average daily dose is 10 mg ursodeoxycholic acid per 1 kg of body weight in 2 divided doses for 2 weeks to 2 months. If necessary, the course of treatment must be repeated. The dosage regimen is determined by the doctor.

Calculation of the daily number of capsules depending on the patient's body weight and the recommended dose of the drug per 1 kg of body weight.

For children from 3 years old - individually (at the rate of 10-20 mg / kg / day).

Active ingredient: ursodeoxycholic acid - 500 mg

Excipients: croscarmellose sodium (primellose) - 16 mg, hydroxypropyl methylcellulose (hypromellose) - 14 mg, magnesium stearate - 5 mg.

The composition of the capsule shell: body: titanium dioxide - 2%, gelatin - up to 100%; cap: titanium dioxide - 1.7434%, sunset yellow dye - 0.4183%, gelatin - up to 100%.

• hypersensitivity to drug components or other bile acids;

• X-ray positive (high calcium) gallstones;

• violations of the contractility of the gallbladder and bile ducts;

• occlusion of the biliary tract;

• frequent episodes of biliary colic;

• cirrhosis of the liver in the stage of decompensation;

• severe hepatic and / or renal failure;

• children's age up to 3 years (for solid dosage forms);

• in children over 3 years of age - an unsuccessful portoenterostomy or cases of failure to restore the normal outflow of bile in children with biliary atresia.

For children under 3 years of age, as well as for patients with difficulty swallowing solid dosage forms, it is recommended to use ursodeoxycholic acid preparations in the form of a suspension.

With caution , the drug should be prescribed for cholelithiasis, cholestatic liver diseases.

Trade name: Ursodez - SZ

Description: Capsules Hard gelatin size є00, opaque, white with a housing and a lid of orange color; the contents of the capsules are granular powder and granules of white or almost white color.

Clinical and pharmacological group: Hepatoprotector with choleretic and cholelitholytic action

Pharmaco-therapeutic group: Hepatoprotective agent

pharmachologic effect

Hepatoprotector. It has a choleretic effect. Reduces the synthesis of cholesterol in the liver, its absorption in the intestine and concentration in bile, increases the solubility of cholesterol in the biliary system, stimulates the formation and excretion of bile. Reduces the lithogenicity of bile, increases the content of bile acids in it. It causes an increase in gastric and pancreatic secretion, enhances the activity of lipase. Has a hypoglycemic effect.

It causes a partial or complete dissolution of cholesterol stones when taken orally, reduces the saturation of bile with cholesterol, which contributes to the mobilization of cholesterol from gallstones.

It has an immunomodulatory effect, affects immunological reactions in the liver: reduces the expression of some antigens on the membrane of hepatocytes, affects the number of T-lymphocytes, the formation of interleukin-2, reduces the number of eosinophils.

Pharmacokinetics

Suction

Ursodeoxycholic acid is absorbed from the small intestine through passive diffusion (about 90%), and from the ileum through active transport. After oral administration in a single dose of 500 mg, Cmax in blood serum after 30, 60, 90 minutes is 3.8 mmol / L, 5.5 mmol / L and 3.7 mmol / L, respectively.

Distribution

Plasma protein binding is high - up to 96-99%. Penetrates the placental barrier. When taken systematically, ursodeoxycholic acid becomes the main bile acid in the blood serum (48% of the total amount of bile acids). The therapeutic effect of the drug depends on the concentration of ursodeoxycholic acid in bile.

Metabolism and excretion

It is metabolized in the liver (clearance at the 'first pass' through the liver) with the formation of taurine and glycine conjugates. The resulting conjugates are secreted into bile.

About 50-70% of the total dose of the drug is excreted by bile. A small amount of unabsorbed ursodeoxycholic acid enters the large intestine, where it is degraded by bacteria (7-dehydroxylation); the resulting lithocholic acid is partially absorbed from the large intestine, but is sulfated in the liver and rapidly excreted in the form of a sulfolitocholylglycine or sulfolitocholyltaurin conjugate.

Indications

• dissolution of cholesterol stones with a functioning gallbladder;

• primary biliary cirrhosis of the liver in the absence of signs of decompensation;

• chronic hepatitis of various origins;

• primary sclerosing cholangitis;

• cystic fibrosis (cystic fibrosis);

• non-alcoholic steatohepatitis;

• alcoholic liver disease;

• biliary dyskinesia.

Dosage regimen

The drug is taken orally.

Dissolving cholesterol gallstones

The recommended (approximate) dose is 10 mg of ursodeoxycholic acid per 1 kg of body weight per day. The drug must be taken daily in the evening, before bedtime (the capsules are not chewed), with a small amount of liquid.

It usually takes 6-24 months to dissolve gallstones. 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 recurrent cholelithiasis, it is recommended to take the drug for several months after the stones dissolve.

Symptomatic treatment of primary biliary cirrhosis

The daily dose depends on body weight and ranges from 1 to 3 capsules (500 mg) (approximately 10 to 15 mg ursodeoxycholic acid per 1 kg of body weight) in 2-3 doses, the first 3 months of treatment. After improving the functional parameters of the liver, the daily dose can be applied 1 time in the evening. The duration of the course of treatment is not limited. In rare cases, at the beginning of treatment, clinical symptoms may worsen (itching becomes more frequent). In this case, you should reduce the daily dose (up to 250 mg), and then gradually increase it (weekly increasing the daily dose) until the recommended dosage regimen is reached.

Chronic hepatitis of various origins, non-alcoholic steatohepatitis and alcoholic liver disease

The average daily dose is from 10 to 15 mg of ursodeoxycholic acid per 1 kg of body weight in 2-3 doses. The duration of therapy is 6-12 months or more.

Primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis)

For primary sclerosing cholangitis: 12-15 mg / kg / day (up to 20 mg / kg / day) in 2-3 doses. The duration of use is from 6 months to several years.

With cystic fibrosis (cystic fibrosis): 20-30 mg / kg / day in 2-3 doses. The duration of use is from 6 months to several years.

Biliary dyskinesia

The average daily dose is 10 mg ursodeoxycholic acid per 1 kg of body weight in 2 divided doses for 2 weeks to 2 months. If necessary, the course of treatment must be repeated. The dosage regimen is determined by the doctor.

Calculation of the daily number of capsules depending on the patient's body weight and the recommended dose of the drug per 1 kg of body weight.

For children from 3 years old - individually (at the rate of 10-20 mg / kg / day).

Side effect

From the digestive system: diarrhea, nausea, pain in the epigastric region and right hypochondrium, calcification of gallstones, increased activity of hepatic transaminases.

In the treatment of primary biliary cirrhosis, transient decompensation of liver cirrhosis may occur, which disappears after discontinuation of the drug.

Others: allergic reactions.

Contraindications for use

• hypersensitivity to drug components or other bile acids;

• X-ray positive (high calcium) gallstones;

• violations of the contractility of the gallbladder and bile ducts;

• occlusion of the biliary tract;

• frequent episodes of biliary colic;

• cirrhosis of the liver in the stage of decompensation;

• severe hepatic and / or renal failure;

• children's age up to 3 years (for solid dosage forms);

• in children over 3 years of age - an unsuccessful portoenterostomy or cases of failure to restore the normal outflow of bile in children with biliary atresia.

For children under 3 years of age, as well as for patients with difficulty swallowing solid dosage forms, it is recommended to use ursodeoxycholic acid preparations in the form of a suspension.

With caution , the drug should be prescribed for cholelithiasis, cholestatic liver diseases.

Application during pregnancy and lactation

The drug is contraindicated during pregnancy and lactation (breastfeeding).

Application for violations of liver function

The drug is contraindicated in severe liver dysfunction, liver cirrhosis in the stage of decompensation.

The drug should be prescribed with caution for cholestatic liver diseases.

Application for impaired renal function

The drug is contraindicated in severe renal impairment.

Application in children

The use of the drug in the form of capsules is contraindicated in children under 3 years of age.

The drug is not prescribed for children weighing up to 34 kg.

special instructions

The use of the drug UrsodezЃ should be carried out under the supervision of a physician.

During the first 3 months of treatment, the functional parameters of the liver (transaminases, alkaline phosphatase and GGT) in the blood serum should be monitored every 4 weeks, and then every 3 months. 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 treatment.

Application for dissolving cholesterol gallstones

In order to assess the progress in treatment, as well as for the timely detection of signs of calcification of stones, the gallbladder should be visualized (oral cholecystography) with an examination of the blackouts in the standing and supine position (ultrasound) 6-10 months after the start of treatment. If the gallbladder cannot be visualized on x-rays or in case of calcification of stones, weak contractility of the gallbladder or frequent attacks of colic, the drug UrsodezЃ should not be used.

Treatment of 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.

Long-term therapy with high doses of ursodeoxycholic acid (28-30 mg / kg / day) can lead to the development of serious side effects in patients with primary sclerosing cholangitis.

In patients with diarrhea, the dose of the drug should be reduced. If diarrhea persists, treatment should be discontinued.

Influence on the ability to drive vehicles and mechanisms

Influence on the ability to drive vehicles and mechanisms has not been identified.

Overdose

No cases of overdose have been identified. In case of an overdose, symptomatic treatment is performed.

Drug interactions

 олестирамин, колестипол и антациды, содержащие алюмини¤ гидроксид или смектит (алюмини¤ оксид), снижают абсорбцию урсодезоксихолевой кислоты в кишечнике и, таким образом, уменьшают ее поглощение и эффективность. ?сли же применение препаратов, содержащих хот¤ бы одно из этих веществ, ¤вл¤етс¤ необходимым, их нужно принимать минимум за 2 ч до приема препарата ”рсодезЃ.

”рсодезоксихолева¤ кислота может усилить всасывание циклоспорина из кишечника. ѕоэтому у пациентов, принимающих циклоспорин, следует проверить концентрацию циклоспорина в крови и скорректировать дозу циклоспорина в случае необходимости.

¬ отдельных случа¤х ”рсодезЃ может снижать всасывание ципрофлоксацина.

Lipid-lowering drugs (especially clofibrate), estrogens, neomycin, or gestagens increase the saturation of bile with cholesterol and may reduce the ability to dissolve cholesterol gallstones.

Storage conditions

The drug should be stored out of the reach of children, protected from light at a temperature not exceeding 25 ? C.

Shelf life

Shelf life is 3 years.

Terms of sale

The drug is available with a prescription.

Contacts for inquiries

NORTH STAR NAO (Russia)

111524 Moscow
st. Electrode, d. 2, bldg. 34, pom. 47
Tel./fax: (495) 137-80-22