ursodeoxycholic acid | Exhol tablets are covered.pl.ob. 500 mg 50 pcs.

Release form

Capsules.

Packing

Capsules, 500 mg. In a blister strip packaging of PVC film and aluminum foil printed varnished 10 pcs. 5 blister packs of 10 pcs. in a pack of cardboard.

Pharmacological action

Exhol - hepatoprotective agent, has a choleretic effect. It reduces the synthesis of cholesterol in the liver, its absorption in the intestine and concentration in 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 in it, causes an increase in gastric and pancreatic secretion, enhances lipase activity, has a hypoglycemic effect. Causes partial or complete dissolution of cholesterol stones during enteral use, reduces the saturation of bile with cholesterol, which helps mobilize cholesterol from gallstones. It has an immunomodulatory effect, affects the 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

Hepatoprotective agent also has choleretic, cholelitholytic, hypolipidemic, hypocholesterolemic and some immunomodulatory effects. Having high polar properties, ursodeoxycholic acid (UDCA) forms non-toxic mixed micelles with apolar (toxic) bile acids, which reduces the ability of gastric reflux to damage cell membranes with biliary reflux gastritis and reflux esophagitis. In addition, UDCA forms binary molecules capable of being incorporated into the cellmembranes of hepatocytes, cholangiocytes, gastrointestinal epithelial cells, stabilize them and make them immune to the action of cytotoxic micelles. By reducing the concentration of bile acids toxic to the liver cell and stimulating bicarbonate-rich choleresis, UDCA effectively helps resolve intrahepatic cholestasis. Reduces the saturation of bile with cholesterol due to the inhibition of its absorption in the intestine, suppression of synthesis in the liver and lower secretion into bile, increases the solubility of cholesterol in bile, forming liquid crystals with it reduces the lithogenic index of bile. The result is the dissolution of cholesterol gallstones and the prevention of the formation of new calculi. The immunostimulating effect is due to including inhibition of the expression of HLA-1 antigens on hepatocyte membranes and HLA-2 on cholangiocytes, normalization of the natural killer activity of lymphocytes. Significantly delays the progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis and alcoholic steatohepatitis reduces the risk of varicose veins of the esophagus. UDCA slows down the processes of premature aging and cell death (including hepatocytes, cholangiocytes).

UDCA is absorbed in the small intestine due to passive diffusion (about 90%), and in the ileum through active transport. Cmax in blood plasma when ingested 50 mg after 30, 60, 90 min - 3.8, 5.5 and 3.7 mmol / l, respectively. Tmax - 1-3 hours. Communication with plasma proteins is high - up to 96–99%. Penetrates through the placental barrier. With systematic administration, UDCA becomes the main bile acid in the blood serum and makes up about 48% of the total amount of bile acids in the blood. The therapeutic effect of the drug depends on the concentration of UDCA in bile. It is metabolized in the liver (clearance during the initial passage through the liver) into taurine and glycine conjugates. The resulting conjugates are secreted into the bile. About 50–70% of the total dose of the drug is excreted by bile. A small amount of non-absorbable UDCA enters the large intestine, where it is digested by bacteria (7-dehydroxylation), the resulting lithocholic acid is partially absorbed from the colon, but is sulfated in the liver and rapidly excreted as a sulfolitocholylglycine or sulfolithocholyltaurin conjugate.

Indications

Uncomplicated gallstone disease (biliary sludge, dissolution of cholesterol gallstones in the gallbladder with a functioning gallbladder prevention of recurrence of stone formation after cholecystectomy)

chronic active hepatitis

toxic (including drug) liver damage

alcoholic liver disease

non-alcoholic liver steatosis hepatitis srdlkrdkrdrglid cystic fibrosis (cystic fibrosis) of the liver

biliary dyskinesia

biliary reflux gastritis and reflux esophagitis.

Contraindications

Hypersensitivity

X-ray-positive (high calcium) gallstones

nonfunctioning gallbladder

gastrointestinal fistula

acute cholecystitis

acute cholangitis srdlkrp cirrhosis of the liver cirrhosis of the liver and / or renal failure

obstruction of the biliary tract

empyema gallbladder

children under 3 years of age.

Caution: children aged 3-4 years, as difficulty swallowing capsules.

Use during pregnancy and lactation

Women of childbearing age are advised to use non-hormonal contraceptives during the period of use of the drug.

The use of UDCA during pregnancy is only possible if the expected benefit to the mother outweighs the potential risk to the fetus. There are currently no data on the allocation of UDCA with breast milk.

If necessary, the use of UDCA during lactation should decide on the termination of breastfeeding.

Special instructions

For successful dissolution, it is necessary that the stones be pure cholesterol, no larger than 15-20 mm in size, the gall bladder is filled with stones no more than half and the bile ducts fully retain their function.

When prescribed for the purpose of dissolving gallstones, it is necessary to control the activity of hepatic transaminases and alkaline phosphatase (ALP), gamma-glutamintransferase (GGT), and bilirubin concentration. Cholecystography should be performed every 4 weeks in the first 3 months of treatment, then every 3 months. Monitoring the effectiveness of treatment is carried out every 6 months during an ultrasound during the first year of therapy.

While maintaining elevated levels, the drug should be discontinued. After the stones are completely dissolved, it is recommended to continue using them for at least 3 months, in order to facilitate the dissolution of stone residues, the sizes of which are too small for their detection and for the prevention of recurrence of stone formation. If, within 6-12 months after the start of therapy, partial dissolution of stones did not occur, it is unlikely that the treatment will be effective. Detection of non-visualizable gallbladder during treatment is evidence that complete dissolution of stones did not occur and treatment should be discontinued.

Composition

1 capsule contains: active substance:

ursodeoxycholic acid 500 mg

excipients:

silicon dioxide colloidal (Aerosil A-200 or A-300),

calcium hydrogen phosphate dihydrate, srdlpdp 90 or collidone 90 F),

lactose monohydrate (milk sugar)

hard gelatin capsule composition:

body - titanium dioxide,

gelatin cap - titanium dioxide,

gelatin, indigo carmine

.

Dosage and administration

Inside, without chewing, with plenty of water.

Diffuse liver diseases, cholelithiasis (cholesterol gallstones and biliary sludge): Exhol® is prescribed continuously for a long time (from several months to several years) in a daily dose of 10 mg / kg to 12-15 mg / kg (2–5 caps.). Duration of administration for dissolving stones - until complete dissolution, plus another 3 months for the prevention of relapse of stone formation. In case of diffuse liver diseases, the daily dose of the Exhol® preparation is divided into 2-3 doses, the capsules are taken with food. In gallstone disease, the entire daily dose is taken once at night.

Biliary reflux gastritis and reflux esophagitis: the drug is prescribed at 250 mg / day (1 caps.), before bedtime. The course of treatment is from 10-14 days to 6 months, if necessary - up to 2 years.

After cholecystectomy, to prevent re-cholelithiasis: the recommended dose is 250 mg 2 times a day for several months.

Toxic, drug-induced liver damage, alcoholic liver disease and atresia of the biliary tract: the daily dose is set at the rate of 10-15 mg / kg in 2-3 doses. The duration of therapy is 6-12 months or more.

Primary biliary cirrhosis: the drug is prescribed at a rate of 10-15 mg / kg / day (if necessary, up to 20 mg / kg) in 2-3 doses. The duration of therapy is from 6 months to several years.

Primary sclerosing cholangitis: 12–15 mg / kg / day (up to 20 mg / kg) in 2–3 doses. The duration of therapy is from 6 months to several years.

Non-alcoholic steatohepatitis: 13–15 mg / kg / day in 2–3 doses. The duration of therapy is from 6 months to several years.

Cystic fibrosis: the dose is set at the rate of 20–30 mg / kg / day (up to 20 mg / kg) in 2–3 doses. The duration of therapy is from 6 months to several years. For children over 3 years of age, the dose of the drug is prescribed individually, at the rate of 10-20 mg / kg / day.

Side effects

Back pain, nausea, vomiting, diarrhea (may be dose-dependent), constipation, transient (transient) increase in liver transaminase activity, allergic reactions, rarely - calcification of gallstones, exacerbation of previously existing psoriasis, alopecia.

Drug Interactions

Antacids containing aluminum and ion exchange resins (colestyramine) reduce the absorption of the drug.

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

Overdose

No overdose has been detected. In case of overdose, symptomatic treatment is performed.

Storage Conditions

Store in a dry, dark place at a temperature not exceeding 25 РC.

Keep out of the reach and sight of children.

Shelf life

3 years.

Deystvuyushtee substance

Ursodezoksiholevaya Chisloth

dosage form

tablets

Possible product names

Exhol tablets are coated. 500 mg 50 pcs.

Kanonfarma, Russia