Ursoliv - instructions for use, dose, side effects, contraindications

Excipients: lactulose 300.0 mg, povidone low molecular weight K17 7.5 mg, magnesium stearate 4.5 mg, talc 6.0 mg, cellulose microcrystalline to obtain a capsule content of 600.0 mg.

capsules are hard gelatinous: body: titanium dioxide 2.00%, gelatin up to 100%.

cover: dye azorubin (E 122) 0.05%, titanium dioxide 1.00%, gelatin up to 100%.

Description:Hard gelatin capsules No. 00 with a white casing and a pink lid. The contents of the capsules are a granular powder of white or almost white color.

Pharmacotherapeutic group:Hepatoprotective agent

ATX: & nbsp

A.05.A.A Preparations of bile acids

Pharmacodynamics:

Has hepatoprotective, choleretic, cholelitolitic, hypolipidemic, hypocholesterolemic and some immunomodulating act.

In studies in vitro shown, that ursodeoxycholic acid (UDCA) has a direct protective effect on liver cells and reduces the hepatotoxicity of hydrophobic bile salts.

The main effects of UDCA on cholesterol metabolism include: lowering cholesterol secretion, reducing its intestinal absorption, and stimulating the release of cholesterol from cholesterol stones into bile. UDCA, inhibiting GMC-CoA reductase, also has a moderate inhibitory effect on the synthesis of cholesterol in the liver, Increases the solubility of cholesterol in the biliary system. Causes partial or complete dissolution of cholesterol gallstones with enteral application, reduces bile saturation with cholesterol, Stimulates the formation and release of bile, accelerates the excretion of toxic bile acids through the intestine. When administered orally, the proportion of UDCA in the common pool of bile acids increases significantly; UDCA competes with other bile acids in the course of absorption in the small intestine, as well as through penetration of the hepatocyte membrane, which leads to a decrease in the absorption of toxic bile acids in the intestine and their entry into the liver, preventing their cytopathogenic action.

It reduces the lithogenicity of bile, increases the concentration of bile acids in it, causes an increase in gastric and pancreatic secretion, increases lipase activity, and has a hypoglycemic effect.

Influences immunological reactions, reducing the pathological expression of antigens of the main histocompatibility complex HLAI on hepatocytes and HLA II on cholangiocytes, suppresses the production of interleukin 2, reduces the number of eosinophils.

Pharmacokinetics:

UDCA is absorbed in the small intestine (about 90%), with the maximum concentration (Cmah) in the blood plasma when taking the drug inside at a dose of 250 mg is about 3.3 μg / ml, the time to reach the maximum concentration - about 2 hours.

Binding to plasma proteins of unconjugated UDCA in healthy people is at least 70%. Penetrates through the placental barrier. With systematic administration in doses of 13-15 mg / kg / day, UDCA becomes the main bile acid in the serum and accounts for 30 to 50% of the total bile acid content in the blood. The therapeutic effect of the drug depends on the concentration of UDCA in the bile.

Metabolised in the liver with conversion to taurine and glycine conjugates, which are secreted in bile. About 50-70% of the dose taken internally is excreted with bile. Excretion in urine does not exceed 1%. A small amount of non-sucked after oral administration of UDCA enters the large intestine,where it undergoes cleavage by bacteria (7-dehydroxylation); the resulting lithocholic acid is partially absorbed from the colon, sulphated in the liver and rapidly excreted as a sulfolithocholylglycine or sulfolitocholyltaurine conjugate.

Indications:

- Primary biliary cirrhosis in the absence of signs of decompensation (symptomatic therapy);

- Dissolution of small and medium cholesterol stones with a functioning gallbladder;

- Biliary reflux-gastritis;

- Chronic hepatitis of various genesis;

- Primary sclerosing cholangitis;

- Cystic fibrosis (cystic fibrosis);

- Non-alcoholic steatohepatitis;

- Alcoholic liver disease;

- Biliary dyskinesia.

Contraindications:

The size of cholesterol stones in the gall bladder is more than 20 mm.

The presence of radiopaque (with a high content of calcium) gallstones and the common bile duct.

Atrophy of the gallbladder with cholelithiasis, a dysfunctional gallbladder. Obstruction of biliary tract.

Acute inflammatory diseases of the gallbladder, bile ducts and intestines.

Cirrhosis in the stage of decompensation.

Pronounced hepatic and renal insufficiency.

Pancreatitis (active phase).

Hypersensitivity to the drug.

Pregnancy, lactation.

Adults and children weighing up to 34 kg (for this dosage form).

Dosing and Administration:

Inside. With difficulty swallowing, the capsule can be opened and taken up with its contents, squeezed with enough liquid.

Dissolution of cholesteric gallstones:

Capsules are taken in the evening, before going to bed, with a sufficient amount of liquid. Approximately 10 mg per 1 kg of body weight daily, which corresponds to:

2 capsules of Ursoliv® in patients with body weight up to 60 kg;

3 capsules of Ursoliv® in patients with body weight up to 80 kg;

4 capsules of Ursoliv® in patients with body weight up to 100 kg;

5 capsules of the drug Ursoliv® in patients with a body weight of more than 100 kg.

Duration of treatment is 6-12 months.

For the prevention of repeated formation of stones, it is recommended to take the drug for several months after the dissolution of the stones.

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).

The drug is taken with food, squeezed with enough liquid.

The following application mode is recommended:

Weight bodies	Daily dose	In the morning	In the afternoon	Ve Th rum
34-50 kg	2 capsules	1		1
51-65 kg	3 capsules	1	1	1
66-85 kg	4 capsules	1	1	2
86-110 kg	5 capsules	1	2	2
Over 110 kg	6 capsules	2	2	2

For the treatment of biliary reflux gastritis:

1 capsule 1 time per day before bedtime. The course of treatment - from 10-14 days to 6 monthsand, if necessary, up to 2 years.

In chronic hepatitis of various genesis (toxic, medicinal, etc.), non-alcoholic fatty liver disease, incl. nonalcoholic 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.

With primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis):

The average daily dose is 12-15 mg / kg; if necessary, the average daily dose can be increased to 20-30 mg / kg in 2-3 doses. The duration of therapy is from 6 months to several years.

When dyskinesia of the bile ducts is hypokinetic:

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

Side effects:

From the digestive system: nausea, vomiting, pain in the epigastric region and right hypochondrium, constipation, transient increase in the activity of "liver" transaminases; rarely - diarrhea (can be dose-dependent), calcification of gallstones.

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

Other: headache, malaise, myalgia, dizziness, allergic reactions (pruritus, urticaria, angioedema), exacerbation of previously existing psoriasis, alopecia.

Overdose:

Cases of overdose UDCA have not been described to date.

Interaction:

When combined, antacids containing aluminum and ion exchange resins (colestramine), reduce the absorption of UDCA.

With the simultaneous use of lipid-lowering drugs (especially clofibrate), estrogens, neomycin or progestogens (oral contraceptives) increase bile saturation with cholesterol and may reduce the ability of ursodeoxycholic acid to dissolve cholesterol gallstones.

With the simultaneous use of UDCA can increase the absorption of cyclosporine.

Special instructions:

To dissolve gallstones UDCA stones must be cholesterol (not radiopaque), a size of not more than 15-20 mm. In this case, the gallbladder should remain functional, and the permeability of the cystic and common bile ducts should be preserved.

When appointing to dissolve gallstones, it is necessary every month, and then every 3 months. conduct a biochemical blood test to determine the activity of "liver" transaminases, alkaline phosphatase, gamma-glutamyl transpeptidase, as well as the concentration of bilirubin. If the increased indices remain, the drug should be discontinued.

To monitor the effectiveness of treatment is recommended every 6 months. conduct X-ray and ultrasound examination of bile ducts.

When calcification of gallstones, violation of the contractility of the gallbladder or frequent attacks of biliary colic, treatment should be discontinued. If within 6-12 months after the beginning of therapy of partial dissolution of concrements did not occur, it is unlikely that the treatment will be effective. Detection during treatment of a nonvisualizable gallbladder is evidence that no complete dissolution of the calculi has occurred, and treatment should be discontinued.

After complete dissolution of the stones, to avoid relapse, it is recommended to continue the use of ursodeoxycholic acid, for 3 months.

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

The drug does not adversely affect the ability to drive vehicles and / or other mechanisms.

Form release / dosage:

Capsules 250 mg.

Packaging:

10 capsules per contour cell packaging made of polyvinylchloride film and aluminum foil printed lacquered.

10, 20, 30, 50, 100 capsules in plastic bottles with a screw cap or polymer can with a screw cap.

Each vial or jar, 1, 2, 3, 5 or 10 contour mesh packages together with the instruction for use is placed in a pack of cardboard.

Storage conditions:

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

Shelf life:

4 years

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-009125/10

Date of registration:31.08.2010 / 18.06.2015

Expiration Date:Unlimited

The owner of the registration certificate:AVVA RUS, OJSC AVVA RUS, OJSC Russia

Manufacturer: & nbsp

AVVA RUS, OJSC Russia

Information update date: & nbsp12.07.2016

Illustrated instructions

Instructions

Ursoliv® (Ursoliv®)