Grinterol hard capsules 250 mg. №50

Description

GRINTEROL №50 COMPOSITION
active substance: ursodeoxycholic acid

1 hard capsule contains 250 mg of ursodeoxycholic acid

excipients: corn starch, silicon dioxide, magnesium stearate

capsule (body and lid): titanium dioxide (E 171), gelatin.

GRINTEROL №50 DOSAGE FORM
The capsules are hard.

GRINTEROL №50 MAIN PHYSICAL AND CHEMICAL PROPERTIES
white hard gelatin capsules. Content – white or almost white powder.

PHARMACOLOGICAL GROUP
Drugs used to treat the liver and biliary tract. Drugs used in biliary pathology. ATX code A05A A02.

Drugs used in liver diseases, lipotropic substances. ATX code A05B.

PHARMACOLOGICAL PROPERTIES
Pharmacological.

A small amount of ursodeoxycholic acid was found in human bile.

After oral administration, it reduces the saturation of bile with cholesterol, suppressing its absorption in the intestine and reducing the secretion of cholesterol in the bile. Perhaps due to the dispersion of cholesterol and the formation of liquid crystals, a gradual dissolution of gallstones occurs.

According to modern data, it is believed that the effect of ursodeoxycholic acid in liver diseases and cholestasis is due to the relative replacement of lipophilic, similar washing toxic bile acids with hydrophilic cytoprotective non-toxic ursodeoxycholic acid, an improvement in the secretory capacity of hepatocytes and immunoregulatory processes.

Application for children

Cystic fibrosis

The use of ursodeoxycholic acid can reduce proliferation in the bile ducts, stop the progression of histological changes and even eliminate hepatobiliary changes, provided that therapy is started in the early stages of cystic fibrosis. For greater effectiveness, treatment with ursodeoxycholic acid should be started immediately after the diagnosis of cystic fibrosis is clarified.

Pharmacokinetics.

When administered orally, ursodeoxycholic acid is rapidly absorbed in the small and upper ileum by passive transport, and in the terminal ileum by active transport. The absorption rate is usually 60-80%. In the liver, bile acid undergoes almost complete conjugation with the amino acids glycine and taurine and is then excreted in the bile. The clearance of the first passage through the liver is up to 60%.

Depending on the daily dose and the underlying liver disorder or condition, the more hydrophilic ursodeoxycholic acid accumulates in the bile. At the same time, there is a relative decrease in other more lipophilic bile acids.

Under the influence of intestinal bacteria, there is a partial degradation of up to 7 ketolithocholic and lithocholic acids. Lithoholic acid is hepatotoxic and causes damage to the liver parenchyma in some animal species. In humans, only a small amount of it is absorbed, which is sulfated in the liver and thus detoxified before being excreted in the bile and finally in the feces.

The biological half-life of ursodeoxycholic acid is 3.5-5.8 days.

INDICATIONS
Dissolution of X-ray negative cholesterol gallstones no more than 15 mm in diameter in patients with a functioning gallbladder, despite the presence of gallstone (s) in it.

Treatment of biliary reflux gastritis.

Symptomatic treatment of primary biliary cirrhosis (PBC) in the absence of decompensated liver cirrhosis.

Treatment of hepatobiliary disorders in cystic fibrosis in children aged 6 to 18 years.

CONTRAINDICATIONS
Hypersensitivity to any substance that is part of the drug.

Acute inflammation of the gallbladder or bile ducts.

Obstruction of the bile ducts (blockage of the common bile duct or duct).

Frequent episodes of hepatic colic.

Radiopaque calcified gallbladder stones.

Violation of the contractility of the gallbladder.

Poor result of portoenterostomy or lack of adequate biliary outflow in children with biliary atresia.