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

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; increases gastric and pancreatic secretion, enhances the activity of lipase, has a hypoglycemic effect. Causes partial or complete dissolution of cholesterol stones duringenteral application, reduces the saturation of bile with cholesterol, which contributes to the mobilization of cholesterol from gallstones. Has immunomodulatory effect, affects immunological reactions in the liver reduces the expression of certain antigens on the membrane hepatocytes, 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 gallstones cholesterol stones, 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 (cystic fibrosis), non-alcoholic 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.

Pregnancy and lactation:

The drug is contraindicated during pregnancy and lactation.

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. Duration of treatment is 6-12 months. 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 of Ursodez® every evening before bedtime, washed down with a small amount of water.

The course of treatment is from 10-14 days 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 2 to 6 capsules (about 10 to 15 mg ursodeoxycholic acid per 1 kg of body weight) in 2-3 doses.

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

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

With primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis)

The average daily dose is from 12 to 15 mg ursodeoxycholic acid on 1 kg of body weight; if necessary, the average daily dose can be increased to 20-30 mg per 1 kg of body weight in 2-3 doses. The duration of therapy is 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 from 2 weeks to 2 months. If necessary, the course of treatment should be repeated.

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

Weight	10	12	15	20	30
body, kg	mg / kg / day	mg / kg / day	mg / kg / day	mg / kg / day	mg / kg / day
34-35	1 caps	2 caps	2 caps	3 caps	4 caps
36-40	2 caps	2 caps	2 caps	3 caps	5 caps
41 -45	2 caps	2 caps	3 caps	4 caps	5 caps
45-50	2 caps	2 caps	3 caps	4 caps	6 caps
51-55	2 caps	3 caps	3 caps	4 caps	7 caps
56-60	2 caps	3 caps	4 caps	5 caps	7 caps
61 -65	3 caps	3 caps	4 caps	5 caps	8 caps
66-70	3 caps	3 caps	4 caps	6 caps	8 caps
71-75	3 caps	4 caps	5 caps	6 caps	9 caps
76-80	3 caps	4 caps	5 caps	6 caps	10 caps
81-85	3 caps	4 caps	5 caps	7 caps	10 caps
86-90	4 caps	4 caps	5 caps	7 caps	11 caps
91 -95	4 caps	5 caps	6 caps	8 caps	11 caps
96-100	4 caps	5 caps	6 caps	8 caps	12 caps
101 - 105	4 caps	5 caps	6 caps	8 caps	13 caps
105-110	4 caps	5 caps	7 caps	9 caps	13 caps

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:

In cholelithiasis, treatment effectiveness is monitored every 6 months by X-ray and ultrasound examination of the biliary tract to prevent relapse of cholelithiasis. When cholestatic liver diseases should periodically determine the activity of transaminases, alkaline phosphatase and gamma-glutamyltranspeptidase in the blood serum.

Effect on the ability to drive transp. cf. and fur:There is no evidence of the influence of ursodeoxycholic acid on the ability to drive vehicles and work with mechanisms.

Form release / dosage:

Capsules 250 mg.

Packaging:

10 capsules per contour cell package.

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

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.

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:

5 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LSR-004408/10

Date of registration:18.05.2010 / 19.05.2015

Expiration Date:Unlimited

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)