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

Excipients: silicon dioxide colloid - 2 mg, calcium hydrophosphate dihydrate 29 mg, magnesium stearate 2 mg, povidone K-90 9 mg, lactose monohydrate 38 mg;

hard capsule composition gelatin № 0: body - titanium dioxide 1.18 mg, gelatin 57.82 mg; cap - titanium dioxide 0.74 mg, gelatin 36.26 mg.

Description:Hard gelatin capsules №0, body and lid of white color. The contents of capsules are white or almost white powder. The presence of granules is allowed.

Pharmacotherapeutic group:Hepatoprotective agent

ATX: & nbsp

A.05.A.A Preparations of bile acids

Pharmacodynamics:

Hepatoprotective agent, also has choleretic, cholelitholitic, hypolipidemic, hypocholesterolemic and some immunomodelling action. Possessing 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 double molecules that can be incorporated into cell membranes (hepatocytes, cholangiocytes, gastrointestinal tract epitheliocytes (GIT)), stabilize them and render them immune to the action of cytotoxic micelles. Reducing the concentration of toxic to the hepatic cell bile acids and stimulating choleresis, rich in bicarbonates, UDCA effectively contributes to the resolution of intrahepatic cholestasis. Reduces the saturation of bile with cholesterol due to inhibition of its absorption in the intestine, suppression of synthesis in the liver and a decrease in secretion in bile; increases the solubility of cholesterol in bile, forming with it liquid crystals; reduces the lithogenic bile index. The result is the dissolution of cholesterol gallstones and the prevention of the formation of new concrements. Immunostimulating effect due to inhibition of expression of antigens HLA-1 on membranes of hepatocytes and HLA-2 on cholangiocytes, normalization of the natural killer activity of lymphocytes, etc. Reliably delay the progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis and alcoholic steatohepatitis; reduces the risk of developing varicose veins of the esophagus.UDCA slows down the processes of premature aging and cell death (hepatocytes, cholangiocytes, etc.).

Pharmacokinetics:

UDCA is absorbed in the small intestine due to passive diffusion (about 90%), and in the ileum through active transport. The maximum concentration in the blood plasma (Cmah) when administered 50 mg after 30, 60, 90 minutes - 3.8 mmol / l, 5.5 mmol / l and 3.7 mmol / l, respectively. FROMmAch is achieved in 1-3 hours. The connection with plasma proteins is high - up to 96-99%. Penetrates through the placental barrier. With systematic admission, UDCA becomes the main bile acid in the blood serum and is 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 the bile.

Metabolised in the liver (clearance during primary passage through the liver) into taurine and glycine conjugates. The resulting conjugates are secreted in bile. About 50-70% of the total dose of the drug is excreted by bile. A small amount of non-absorbed UDCA enters the large intestine, where it undergoes cleavage by bacteria (7-dehydroxylation); the resulting lithocholic acid is partially absorbed from the colon,but sulfated in the liver and rapidly excreted as a sulfolitocholylglycine or sulfolitocholyltaurine conjugate.

Indications:

- Uncomplicated cholelithiasis (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 medicinal) lesions of the liver;

- alcoholic liver disease;

- non-alcoholic steatohepatitis;

- primary biliary cirrhosis;

- primary sclerosing cholangitis;

- cystic fibrosis (cystic fibrosis) of the liver;

- biliary dyskinesia;

- biliary reflux gastritis and reflux esophagitis.

Contraindications:

Hypersensitivity, x-ray positive (high calcium content) gallstones, dysfunctional gallbladder, bile-gastric fistula, acute cholecystitis, acute cholangitis, decompensated hepatic cirrhosis, acute infectious diseases of the gallbladder, bile duct and intestine, expressed hepatic and / or renal insufficiency, obturation of the biliary tract, empyema of the gallbladder, children's age of up to 3 years.

Carefully:

Although UDCA does not have age limitations in use, Exoll® capsules are used with caution in children aged 3 to 4 years, possible difficulty in swallowing capsules.

Pregnancy and lactation:

Women of childbearing age are advised to use non-hormonal contraceptives during the period of drug use. The use of UDCA during pregnancy is possible only if the expected benefit for the mother exceeds the potential risk to the fetus. Data on the isolation of UDCA with breast milk are currently not available. If UDCA is necessary in the lactation period, the question of stopping breastfeeding should be addressed.

Dosing and Administration:

Inside, not liquid, squeezed enough water.

In cases of diffuse liver disease, cholelithiasis (cholesterol gallstones and biliary sludge) Exoll® is administered continuously for a long time (from several months to several years) at a daily dose of 10 mg / kg body weight to 12-15 mg / kg ( 2-5 capsules). Duration of admission for dissolution of stones - until complete dissolution, plus 3 more months to prevent recurrence of stone formation.In case of diffuse liver diseases, the daily dose of Exxhol® is divided into 2-3 doses, the capsules are taken with food. With cholelithiasis, the whole daily intake is taken once for the night. The duration of the drug to dissolve the stones - until complete dissolution, and then 3 more months to prevent recurrence of stone formation.

With biliary reflux gastritis and reflux esophagitis, the drug is prescribed 250 mg (1 capsule) per day, at bedtime. The course of treatment - from 10-14 days to 6 months, if necessary - up to 2 years.

After cholecystectomy, for the prevention of recurrent cholelithiasis, the recommended dose is 250 mg twice a day for several months.

With toxic, medicinal 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 divided doses. The duration of therapy is 6-12 months or more.

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

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

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

In cystic fibrosis, the dose is set at a 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 the age of 3 years, the dose is prescribed individually at the rate of 10-20 mg / kg / day.

Side effects:

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

Overdose:

Cases of an overdose have not been revealed. In case of an overdose, symptomatic treatment is performed.

Interaction:

Antacids containing aluminum and ion-exchange resins (colestramine), reduce the absorption of the drug.

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:

To successfully dissolve it is necessary that the stones are pure cholesterol, with a size not exceeding 15-20 mm, the gallbladder is filled with stones no more than half and the bile ducts fully retained their function.

At the appointment with the purpose of dissolution of gallstones, it is necessary to control the activity of "liver" transaminases and alkaline phosphatase (GF), gamma-glutamine transferase (GGT), bilirubin concentration. Cholecystography should be performed every 4 weeks in the first 3 months of treatment, then every 3 months. Control the effectiveness of treatment every 6 months during ultrasound during the first year of therapy.

If the increased indices remain, the drug should be discontinued. After complete dissolution of the calculus, it is recommended to continue use for at least 3 months in order to promote the dissolution of stone remains that are too small to detect and to prevent the recurrence of stone formation. 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.

Form release / dosage:

Capsules 250 mg.

Packaging:

For 10 or 15 capsules in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1, 3, 5, 10 contour cell packs of 10 capsules or 2, 4, 6 contiguous cell packs of 15 capsules with instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005648/09

Date of registration:14.07.2009 / 15.04.2015

Expiration Date:Unlimited

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Information update date: & nbsp12.07.2016

Illustrated instructions

Instructions

Exxol® (Exhol)