Ursodez - instructions for use, doses, side effects, contraindications

active substance: ursodeoxycholic acid 250 mg Excipients: starch pregelatinized (starch 1500) - 73.0 mg, silicon dioxide colloid (aerosil) 5.0 mg, magnesium stearate 2.0 mg

shell capsules: body and lid: titanium dioxide - 2.1 118%, gelatin - up to 100%;

for a dosage of 500 mg:

active substance: ursodeoxycholic acid - 500 mg Excipients: croscarmellose sodium (impellosis) - 16.0 mg, hydroxypropylmethylcellulose (hypromellose) - 14.0 mg, magnesium stearate 5.0 mg

shell capsules: body: titanium dioxide - 2.0%, gelatin - up to 100%, lid: titanium dioxide - 1.7434%, dye sunset yellow - 0.4183%, gelatin - up to 100%.

Description:

For a dosage of 250 mg

Solid, white, opaque gelatin capsules. The capsule size is No. 0. The contents of the capsules are white or almost white powder.

For a dosage of 500 mg

Solid, opaque gelatin capsules No. 00: white body with an orange lid. The contents of the capsules are a granular powder and granules of white or almost white color.

Pharmacotherapeutic group:Hepatoprotective agent

ATX: & nbsp

A.05.A.A Preparations of bile acids

Pharmacodynamics:

Hepatoprotective agent, has a cholagogue effect. Reduces the synthesis of cholesterol in the liver, its absorption in the intestine and concentration in the bile, increases the solubility of cholesterol in the biliary system, stimulates the formation and secretion of bile. Reduces the lithogenicity of bile, increases the content of bile acids; causes an increase in gastric and pancreatic secretion, increases lipase activity, and has a hypoglycemic effect. Causes partial or complete dissolution of cholesterol stones when applied 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 certain antigens on the hepatocyte membrane, affects the number of T-lymphocytes, the formation of interleukin-2, reduces the number of eosinophils.

Pharmacokinetics:

Ursodeoxycholic acid (UDCA) is absorbed in the small intestine due to passive diffusion (about 90%), and in the ileum through active transport.After oral administration in a single dose (500 mg), the maximum concentration in the blood serum (Cmah) after 30, 60, 90 minutes is 3.8, 5.5, 3.7 mmol / l, respectively. The connection with plasma proteins is high - up to 96-99%. Penetrates through the placental barrier. With systematic admission ursodeoxycholic acid becomes the main bile acid serum (48% of the total bile acids). The therapeutic effect of the drug depends on the concentration of UDCA in the bile.

Metabolised in the liver (clearance at the "primary passage" through the liver) into taurine and glycine conjugates. The resulting conjugates are secreted in bile. About 50-70% of the total dose is excreted through the intestine. A small amount of unsweetened ursodeoxycholic acid enters the large intestine, where it undergoes cleavage by bacteria (7-dehydroxylation); the resulting lithocholic acid is partially absorbed from the colon but is sulfated in the liver and is rapidly excreted as a sulfolithocholylglycine or sulfolithocholyltaurine conjugate.

Indications:

Dissolution of small and medium cholesterol stones with a functioning gallbladder, biliary reflux gastritis, primary biliary cirrhosis in the absence of signs of decompensation (symptomatic treatment).

Chronic hepatitis of various genesis, primary sclerosing cholangitis, cystic fibrosis (mucoviscidosis), nonalcoholic steatohepatitis, alcoholic liver disease, biliary dyskinesia.

Contraindications:

- X-ray positive (high in calcium) gallstones;

- Non-functioning gallbladder;

- Acute inflammatory diseases of the gallbladder, bile ducts and intestines;

- Cirrhosis of the liver in the stage of decompensation;

- Expressed violations of the liver, kidneys, pancreas;

- Hypersensitivity to the components of the drug;

- Adults and children weighing up to 34 kg;

- Children under 3 years old, for this dosage form.

Carefully:

Use with caution under the following conditions:

with cholelithiasis, with cholestatic diseases of the liver (cf. section "Special instructions").

Pregnancy and lactation:

The drug is contraindicated during pregnancy and breastfeeding.

Dosing and Administration:

Inside.

Dissolution of cholesteric gallstones

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

To dissolve gallstones, it is usually required 6-24 months. If after 12 months of treatment the size of the stones does not decrease, then the treatment should be stopped.

The effectiveness of treatment should be evaluated every 6 months with ultrasound or radiography. During the interim survey, it should be assessed whether stone calcification has occurred during the past period. In the case of calcification of stones, treatment should be discontinued.

For the prevention of repeated cholelithiasis, the use of the drug is recommended for several months after the dissolution of the stones.

Treatment of biliary reflux gastritis

1 capsule (250 mg) of Ursodez® every evening before bedtime, with a small amount of water.

The course of treatment from 10-14 days up to 6 months, if necessary - up to 2 years. Symptomatic treatment of primary biliary cirrhosis

The daily dose depends on the body weight and is from 1 to 3 capsules (500 mg) or from 2 to 6 capsules (250 mg) (about 10 to 15 mg ursodeoxycholic acid per 1 kg of body weight) in 2 to 3 doses, the first 3 month of treatment. After improving the functional parameters of the liver, the daily dose can be applied once in the evening.The duration of the course of treatment is not limited. In rare cases, clinical symptoms may worsen at the beginning of treatment (itching may occur). 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 dosing regimen is reached.

With chronic hepatitis of various genesis, non-alcoholic steatohepatitis and alcoholic liver disease

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

With primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis)

With the primary sclerosing cholangitis: 12-15 mg / kg / day (up to 20 mg / kg) of body weight per day in 2-3 divided doses. Duration of use - from 6 months to several beds.

For cystic fibrosis (cystic fibrosis): 20-30 mg / kg per day in 2-3 times. Duration of use - from 6 months to several years.

With dyskinesia biliary tract

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 should 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

Body weight, kg		10 mg / kg / day		12 mg / kg / day		15 m. g / ct / day		20 mg / kg / day		30 mg / kg / day
34 35		1 caps. 250 mg		2 caps, 250 mg or 1 caps, 500 mg each		2 caps, 250 mg or 1 caps, 500 mg each		3 caps, 250 mg each		4 caps, 250 mg or 2 caps, 500 mg each
36 - 40		2 caps, 250 mg or 1 caps, 500 mg each		2 capsules, but 250 mg or 1 caps, 500 mg each		2 caps, 250 mg or 1 cap, 500 mg each		3 caps, 250 mg each		5 caps, 250 mg each
41 -45		2 caps, 250 mg or 1 caps, 500 mg each		2 caps, 250 mg or 1 caps, 500 mg each		3 capsules, but 250 mg		4 caps, 250 mg or 2 caps, 500 mg each		5 caps, 250 mg each
45 - 50		2 caps, 250 mg or 1 caps, 500 mg each		2 caps, 250 mg or 1 caps, but 500 mg		3 caps, 250 mg each		4 caps, 250 mg or 2 caps, but 500 mg		6 caps, 250 mg or 3 caps, 500 mg each
51 - 55		2 caps, 250 mg or 1 cap, 500 mg each		3 caps, 250 mg each		3 caps, 250 mg each		4 caps, 250 mg or 2 caps, 500 mg each		7 caps, 250 mg each
56-60	2 capsules, but 250 mg or 1 caps, 500 mg each		3 caps, 250 mg each		4 caps, 250 mg or 2 caps, 500 mg each		5 caps, 250 mg each		7 caps, but 250 mg
61-65	3 caps, 250 mg each		3 caps, 250 mg each		4 caps, 250 mg or 2 caps, 500 mg each		5 caps, 250 mg each		8 caps, 250 mg or 4 caps, 500 mg each
66-70	3 caps, 250 mg each		3 caps, 250 mg each		4 caps, but 250 mg or 2 caps, 500 mg each		6 caps, 250 mg or 3 caps, 500 mg each		8 caps, 250 mg or 4 caps, 500 mg each
71-75	3 caps, 250 mg each		4 caps, 250 mg or 2 caps, 500 mg each		5 caps, 250 mg each		6 caps, 250 mg or 3 caps, 500 mg each		9 caps, 250 mg each
76-80	3 caps, 250 mg each		4 caps, 250 mg or 2 caps, 500 mg each		5 caps, 250 mg each		6 caps, 250 mg or 3 caps, 500 mg each		10 caps, 250 mg or 5 caps, 500 mg each
81-85	3 caps, 250 mg each		4 caps, 250 mg or 2 caps, 500 mg each		5 caps, 250 mg each		7 caps, 250 mg each		10 caps, 250 mg or 5 caps, 500 mg each
86-90	4 caps, 250 mg or 2 caps, 500 mg each		4 caps, 250 mg or 2 caps, 500 mg each		5 caps, 250 mg each		7 caps, but 250 mg		11 caps, 250 mg each
91 -95	4 caps, 250 mg or 2 caps, 500 mg each		5 caps, 250 mg each		6 caps, 250 mg or 3 caps, 500 mg each		8 caps, 250 mg or 4 caps, 500 mg each		11 caps, 250 mg each
96- 100	4 caps, 250 mg or 2 caps, 500 mg each		5 caps, 250 mg each		6 caps, 250 mg or 3 caps, 500 mg each		8 caps, 250 mg or 4 caps, 500 mg each		12 caps, 250 mg or 5 caps, 500 mg each
101 - 105	4 caps, 250 mg or 2 caps, 500 mg each		5 caps, 250 mg each		6 caps, 250 mg or 3 caps, 500 mg each		8 caps, 250 mg or 4 caps, 500 mg each		13 caps, 250 mg each
105 - 110	4 caps, 250 mg or 2 caps, but 500 mg		5 caps, 250 mg each		7 caps, 250 mg each		9 caps, 250 mg each		13 caps, 250 mg each

For children from 3 years old

Individually (at the rate of 10-20 mg / kg per day).

Side effects:

Diarrhea, nausea, pain in the epigastric region and right hypochondrium, calcification of gallstones, increased activity of "liver" transaminases, allergic reactions.

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

Overdose:

Cases of an overdose have not been revealed. In case of an overdose, symptomatic treatment is performed.

Interaction:

Kolestyramine, colestipol and antacids, containing aluminum hydroxide or smectite (aluminum oxide), reduce the absorption of ursodeoxycholic acid in the intestine and thus reduce its absorption and efficacy. If the use of drugs containing at least one of these substances is still necessary, they should be taken at least 2 hours prior to taking Ursodez.

Ursodeoxycholic acid can increase the absorption of cyclosporine from the intestine. Therefore, in patients receiving ciclosporin, the doctor should check the concentration of cyclosporine in the blood and adjust the dose of cyclosporine, if necessary.

In some cases, ursodez® can reduce the absorption of ciprofloxacin. Lipid-lowering drugs (especially clofibrate), estrogens, neomycin or progestins increase bile saturation with cholesterol and may decrease the ability to dissolve cholesterol bile stones.

Special instructions:

The drug Ursodez ® should be administered under the supervision of a doctor.During the first 3 months of treatment, liver function tests (transaminases, alkaline phosphatase and gamma-glutamyltranspeptidase) in the blood serum should be monitored every 4 weeks, and then every 3 months.

Control of these parameters allows us to identify violations of liver function in the early stages. Also, this applies to patients in the late stages of primary biliary cirrhosis. In addition, it is possible to quickly determine if the patient is responding to primary biliary cirrhosis for ongoing treatment.

When used to dissolve cholesterol gallstones:

In order to assess the progress in treatment and for the timely detection of signs of calcification of stones, the gallbladder should be visualized (oral cholecystography) with examination of blackouts at the "standing" and "lying on the back" (ultrasound) 6-10 months after the start of the study. If the gallbladder can not be visualized on X-rays or in cases of calcification of stones, weak gallbladder contractility or frequent colic attacks, the Ursodez® drug should not be used.

In the treatment of patients in the late stages of primary biliary cirrhosis: extremely rare casesdecompensation of liver cirrhosis. 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.

Patients with diarrhea should reduce the dosage of the drug. With persistent diarrhea, treatment should be discontinued.

Effect on the ability to drive transp. cf. and fur:

Influence on ability to drive vehicles, mechanisms is not revealed.

Form release / dosage:Capsules 250 mg, 500 mg.

Packaging:

Capsules 250 mg.

10 capsules in a planar cell package.

For 40, 50, 60, 100 and 120 capsules in a can of polymer or a polymer vial.

Each jar or vial, 4, 5, 6, 9, 10 or 12 contour mesh packages together with the instruction for use is placed in a cardboard box.

Capsules 500 mg.

10 capsules in a planar cell package.

For 30, 50 capsules a can of polymer or in a polymer vial.

Each jar, vial or 1, 3, 5 contour mesh packages together with the instruction for use is placed in a cardboard box.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

For a dosage of 250 mg 5 years

For a dosage of 500 mg 3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-003238

Date of registration:08.10.2015

Expiration Date:08.10.2020

The owner of the registration certificate:NORTH STAR, CJSC NORTH STAR, CJSC Russia

Manufacturer: & nbsp

NORTH STAR, CJSC Russia

Information update date: & nbsp12.07.2016

Illustrated instructions

Instructions

Ursodez® (Ursodez)