Grinterol, 0.25 caps 50pcs

Composition

One capsule contains:

Active ingredient:

ursodeoxycholic acid-250.0 mg;

excipients:

corn starch-73.0 mg,

silicon dioxide-5.0 mg,

magnesium stearate-2.0 mg;

capsule (body and lid): titanium dioxide (E 171) – 2%, gelatin – up to 100%.

Description:

Solid gelatin capsules No. 0, white body and lid.

The contents are white or almost white powder.

Pharmacological action

Pharmacodynamics

A hepatoprotective agent, it also has choleretic, cholelitolytic, hypolipidemic, hypocholesterolemic and some immunomodulatory effects.

It is embedded in the hepatocyte membrane, stabilizes its structure and protects the hepatocyte from the damaging effect of bile acid 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, litocholic, deoxycholic, etc. ), 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. It screens nonpolar bile acids (chenodeoxycholic), thereby forming mixed (non-toxic) micelles.

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 excretion of bile. Reduces the lithogenicity of bile, increases the concentration of bile acids in it, causes increased gastric and pancreatic secretion, increases the activity of lipase, and has a hypoglycemic effect. Causes partial or complete dissolution of cholesterol gallstones when applied orally, 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 certain histocompatibility antigens – HLA-1 on the membrane of hepatocytes and HLA-2 on cholangiocytes, affects the number of T-lymphocytes, interleukin 2 formation, reduces the number of eosinophils, suppresses immunocompetent Ig (primarily IgM).

Pharmacokinetics

Absorption from the small intestine is high (about 90%). Penetrates the placental barrier. Cmax When ingested 50 mg after 30,60,90 minutes – 3.8; 5.5; 3.7 mmol/l, respectively. Tsmakh – 1-3 hours. The connection with plasma proteins is high.

It is metabolized in the liver (clearance during “primary passage”through the liver) to taurine and glycine conjugates, which are secreted into the bile. It is excreted by 50-70% through the intestines. A small amount of unabsorbed ursodeoxycholic acid enters the large intestine, where it undergoes cleavage by bacteria (7?dehydroxylation); the resulting litocholic acid is partially absorbed from the colon, but is sulfated in the liver and is quickly excreted as a sulfolitocholylglycine or sulfolitocholyltaurine conjugate.

Indications

The dissolution of small and medium cholesterol stones in a functioning gallbladder

– biliary reflux-gastritis,

primary biliary cirrhosis in the absence of signs of decompensation (symptomatic therapy),

chronic hepatitis of various etiology,

primary sclerosing cholangitis, cystic fibrosis (mucoviscidosis),

– non-alcoholic steatohepatitis,

alcoholic liver disease (ALD),

– biliary dyskinesia.

Contraindications

– Hypersensitivity to the components of the drug;

– roentgenologically (with a high content of CA 2+) gallstones;

– non-functioning gall bladder

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

liver cirrhosis in the stage of decompensation;

– severe hepatic and/or renal failure;

– pancreatitis;

– children’s age up to 3 years(for capsules).

With caution:

Children aged 3 to 4 years should be used with caution, as it may be difficult to swallow capsules.

Side effects

Gastrointestinal disorders: loose stools or diarrhea. In the treatment of primary biliary cirrhosis, acute pain in the right upper abdomen may occur.

Liver and biliary tract disorders: calcification of gallstones. In the treatment of primary biliary cirrhosis, temporary decompensation of liver cirrhosis may occur (it passes after discontinuation of the drug).

Skin and subcutaneous tissue disorders: allergic reactions (including urticaria).

Interaction

Antacids containing aluminum hydroxide, aluminum oxide and ion exchange resins (colestyramine, colestipol) reduce the absorption of ursodeoxycholic acid in the intestine, thus reducing its effectiveness; therefore, these drugs should be used 2 hours before taking ursodeoxycholic acid.

Ursodeoxycholic acid can increase the absorption of cyclosporine from the intestine, so when used simultaneously, the dose of cyclosporine should be adjusted.

Ursodeoxycholic acid may reduce the absorption of ciprofloxacin.

Hypolipidemic drugs (especially clofibrate), estrogens, neomycin or progestins, and oral contraceptives increase the saturation of bile with cholesterol and may reduce the ability to dissolve cholesterol bile stones.

How to take, course of use and dosage

Inside. Capsules are taken in the evening, without chewing, with a small amount of water.

Dissolution of cholesterol gallstones: the average daily dose is 10 mg / kg, which corresponds to:

Body weight (kg)

Number of capsules

Up To 60

2

61-80

3

81-100

4

Over 100

5

The course of treatment is 6-12 months. To prevent the re-formation of stones, it is recommended to take the drug for several more months after the dissolution of the stones.

Treatment of biliary reflux gastritis: one capsule 250 mg 1 time a day in the evening. The course of treatment is from 10-14 days to 6 months, if necessary-up to 2 years.

Symptomatic treatment of primary biliary cirrhosis in the absence of signs of decompensation: 10-15 mg / kg (if necessary – up to 20 mg/kg) per day in 2?3 doses in the first 3 months of treatment. After improving liver parameters, the daily dose can be applied once in the evening.

The following application mode is recommended:

Body weight

(kg)

Daily dose

(number of capsules)

In the morning

During the day

In the evening

47-62

3

1

1

1

63-78

4

1

1

2

79-93

5

1

2

2

94-109

6

2

2

2

Over 100

7

2

2

3

The duration of treatment is unlimited. In rare cases, at the beginning of treatment, clinical symptoms may worsen (pruritus may become more frequent). In this case, you should take one capsule daily, then gradually increase the dosage (weekly increasing the daily dose by one capsule) until the recommended dosage regimen is reached.

Symptomatic treatment of chronic hepatitis of various origins: the daily dose is 10-15 mg / kg in 2-3 doses. The duration of treatment is 6-12 months or more.

Primary sclerosing cholangitis: 12-15 mg / kg (up to 20 mg/kg) of body weight per day in 2?3 receptions. Duration of application-from 6 months to several years.

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

Non-alcoholic steatohepatitis: the average daily dose is 10-15 mg / kg in 2?3 receptions. Duration of application-from 6-12 months or more.

Children aged from 3 years are prescribed individually, at the rate of 10-20 mg / kg per day.

Alcoholic liver disease: the average daily dose is 10-15 mg / kg in 2-3 divided doses. The duration of therapy is 6-12 months or more.

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.

Children and adults with a body weight of less than 47 kg are recommended to use the drug in a suspension of other manufacturers.

Overdose

Cases of overdose of ursodeoxycholic acid are not known.

Special instructions

Treatment should be carried out under the supervision of a doctor.

When prescribing for the purpose of dissolving gallstones, it is necessary to monitor the activity of “hepatic” transaminases and alkaline phosphatase, gamma-glutamyltranspeptidase, and bilirubin concentration. Cholecystography should be performed every 4 weeks for the first 3 months of treatment, and then every 3 months. Monitoring of the effectiveness of treatment should be performed every 6 months during ultrasound examination (ultrasound) during the first year of therapy.

If elevated indicators persist, the drug should be discontinued.

For successful dissolution, it is necessary that the stones are pure cholesterol, no more than 15-20 mm in size, the gallbladder is filled with stones no more than half, and the biliary tract completely retains its function.

After the calculus is completely dissolved, it is recommended to continue the application for at least 3 months, in order to promote the dissolution of calculus residues, the size of which is too small to detect.

If there is no partial dissolution of the calculus within 6-12 months after the start of therapy, it is unlikely that the treatment will be effective.

The detection of a non-visualized gallbladder during treatment is an indication that the calculus has not completely dissolved and treatment should be discontinued.

In patients with diarrhea, the dosage of ursodeoxycholic acid should be reduced. If persistent diarrhea occurs, treatment should be discontinued.

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

Influence on the ability to drive vehicles and mechanisms:

The effect on the ability to drive vehicles and mechanisms was not revealed.

Form of production

Capsules.

Storage conditions

Store at a temperature not exceeding 25 ° C. Keep out of reach of children.

Shelf

life is 2 years. Do not use after the expiration date indicated on the package.

Active ingredient

Ursodeoxycholic acid

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Purpose

For adults, For adults as prescribed by a doctor, For Children as prescribed by a doctor

Indications

Biliary dyskinesia, Cholelithiasis, Cirrhosis of the liver, Alcoholism, Liver damage, Hepatitis