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

Excipients: calcium hydrogen phosphate dihydrate 40 mg, calcium stearate 7 mg, sodium carboxymethyl starch 28 mg, potato starch 33.5 mg, mannitol 58 mg, macrogol (polyethylene glycol 4000) 3.5 mg, povidone K-30 30 mg;

composition of film shell: Fill white with 20 mg, including: hypromellose (hydroxypropylmethylcellulose) 6.75 mg, giprolose (hydroxypropyl cellulose) 6.75 mg, talc 4 mg, titanium dioxide 2.5 mg.

Description:The tablets are oval, with a risk, covered with a film shell of white or almost white color. On a cross-section - white or almost white color.

Pharmacotherapeutic group:Hepatoprotective agent

ATX: & nbsp

A.05.A.A Preparations of bile acids

Pharmacodynamics:

Hepatoprotective agent, also has choleretic, cholelitolitic, hypolipidemic, hypocholesterolemic and some immunomodulating 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 damage cell membranes with biliary reflux gastritis and reflux-esophagitis. In addition, UDCA forms double molecules, capable of being included in the composition of cell membranes (hepatocytes, cholangiocytes, gastrointestinal tract epitheliocytes (GIT)), stabilize them and make them unreceptive to the action of cytotoxic micelle. Reducing the concentration of toxic for the hepatic cell biliary acids and stimulating choleresis, rich in bicarbonates, UDCA is effective contributes to the resolution of intrahepatic cholestasis. Reduces saturation of bile with cholesterol due to inhibition of its absorption in intestine, inhibition 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 Dissolution of cholesterol gallstones and prevention of formation new concrements. Immunostimulating effect due to oppression of antigen expression HLA-1 on membranes of hepatocytes and HLA-2 on cholangiocytes, normalization of natural killer activity 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 expansions 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 administration, UDCA becomes the main bile acid, in the blood serum and accounts for 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 is sulfated in the liver and is rapidly excreted as a sulfolithocholylglycine or sulfolithocholyltaurine conjugate.

Indications:

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

- biliary reflux-gastritis;

- primary biliary cirrhosis in the absence of signs of decompensation (symptomatic treatment);

- chronic hepatitis of various genesis;

- primary sclerosing cholangitis;

- cystic fibrosis (cystic fibrosis);

- non-alcoholic steatohepatitis;

- alcoholic liver disease;

- dyskinesia of bile ducts.

Contraindications:

Hypersensitivity to ursodeoxycholic acid or any of the components of the drug, x-ray positive (high calcium content) gallstones, dysfunctional gallbladder, acute infectious and inflammatory diseases of the gallbladder, bile duct and intestine, cirrhosis of the liver in the stage of decompensation,severe hepatic and / or renal insufficiency, pancreatitis, adults and children weighing up to 34 kg, children under 3 years old for this LF.

Pregnancy and lactation:The use of Exoll® 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 you need to use the drug during breastfeeding, you should decide whether to stop breastfeeding.

Dosing and Administration:

Inside, not liquid, squeezed enough water.

Dissolution of gallstones cholesterol stones

The recommended dose of Exxol® is 10 mg / kg body weight in day.

The entire daily intake is taken once for the night. The course of treatment is 6 - 12 months. To prevent the re-formation of stones is recommended admission drug for a few more months after the dissolution of the stones.

Treatment of biliary reflux gastritis

250 mg per day, before bedtime. The course of treatment - from 10-14 days to 6 months, if necessary - up to 2 years.

Symptomatic treatment of primary biliary cirrhosis

The daily dose depends on the body weight and is 10-15 mg / kg / day (if necessary - up to 20 mg / kg) in 2-3 doses in the first 3 months of treatment. After improving the "hepatic" parameters, the daily dose can be applied once in the evening. The duration of the course of treatment is not limited. In rare cases, at the beginning, clinical symptoms may worsen (itching becomes more frequent). In this case, you should reduce the daily dose, and then gradually increase the dosage (weekly increasing daily dose) until the recommended regimen is reached dosing.

With chronic hepatitis of various genesis, non-alcoholic steatohepatitis, alcoholic liver disease

The drug Exhol® is prescribed in a daily dose of 10-15 mg of ursodeoxycholic acid per 1 kg of body weight in 2-3 divided doses, continuously for a long time (6-12 months or more).

With primary sclerosing cholangitis and cystic fibrosis (cystic fibrosis)

With the primary sclerosing cholangitis: 12-15 mg / kg / day (up to 20 mg / kg) of body weight per day in 2-3 divided doses.

With dyskinesia biliary tract

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.

If it is impossible to perform the dosing regimen, it is recommended to use the capsule dosage form, Exhal, 250 mg.

Children older than 3 years ursodeoxycholic acid is administered individually, at a rate of 10-20 mg / kg / day.

Side effects:

Classification of WHO (World Health Organization) incidence of side effects:

often from ≥1 / 100 to <1/10 of appointments (> 1% and <10%); infrequently - from ≥1 / 1000 to <1/100 of prescriptions (> 0.1% and <1%); rarely from ≥1 / 10,000 to <1/1000 appointments (> 0.01% and <0.1%); very rarely - <1/10000 prescriptions (<0.01%).

From the gastrointestinal tract: often - unformed stool, diarrhea (may be dose-dependent); very rarely - in the treatment of primary biliary cirrhosis, transient decompensation of liver cirrhosis (after the drug is discontinued).

From the liver and biliary tract: very rarely - calcification of gallstones, in the treatment of advanced stages of primary biliary cirrhosis decompensation of liver cirrhosis, which disappears after drug withdrawal.

From the skin: very rarely - allergic reactions (including urticaria).

Overdose:

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

Interaction:

Antacids containing aluminum, ion-exchange resins (colestyramine, colestipol) reduce the absorption of ursodeoxycholic acid. If the use of drugs containing at least one of these substances is still necessary, they must be taken at least 2 hours prior to taking Exoll®.

Ursodeoxycholic acid can enhance the absorption of cyclosporine from the intestine. Therefore, in patients receiving ciclosporin, it is necessary to monitor its concentration in the blood and adjust the dose of cyclosporine, if necessary.

In some cases, Exxhol® may reduce the absorption of ciprofloxacin.

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 gallstones, it is necessary that the stones are pure cholesterol, not more than 15-20 mm in size, the gallbladder should remain functional and be filled with stones no more than half, the bile ducts should fully retain their function.

During the first three months of treatment, it is necessary to monitor the activity of "liver" transaminases, alkaline phosphatase (GF), gamma-glutamine transferase (GGT), serum bilirubin concentrations every 4 weeks, and then every 3 months.

Cholecystography should be performed every 4 weeks in the first 3 months of treatment, in the future - every 3 months. Control of treatment effectiveness should be performed every 6 months during ultrasound and X-ray examination of the biliary tract during the first year of therapy.

Detection during treatment of a nonvisualizable gallbladder is evidence that a complete dissolution of concrements has occurred and treatment should be discontinued. In cases of calcification of stones, weak contractility of the gallbladder or frequent attacks of colic, Exol® should not be used. 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. 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.

Patients with diarrhea should reduce the dosage of the drug. With persistent diarrhea, treatment should be discontinued.

If long-term therapy with high doses of ursodeoxycholic acid (up to 30 mg / kg / day) is necessary, the use of the drug may lead to the development of serious side effects in patients with primary sclerosing hallaMr.gita.

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

When using Exoll®, the effect on the ability to drive vehicles and mechanisms is not revealed.

Form release / dosage:

Tablets, film-coated, 500 mg.

Packaging:

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

For 1, 3, 5, 10 contour cell packs of 10 tablets together with the 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:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002956

Date of registration:14.04.2015

Expiration Date:14.04.2020

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)