Composition, form of production and packaging
Capsules 1 caps.
ursodeoxycholic acid 300 mg
10 pieces. - blisters of aluminum foil and PVC film (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Choludexan is a hepatoprotective agent, it also has choleretic, cholelitholytic, hypolipidemic, hypocholesterolemic and some immunomodulatory effects.
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 refluxesophagitis. In addition, UDCA forms double molecules that can be incorporated into cell membranes (hepatocytes, cholangiocytes, GIT), stabilize them and render them immune to the action of cytotoxic micelles. Reducing the concentration of toxic for 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 lowering 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 is caused by inhibition of HLA-1 antigens expression on hepatocyte membranes and HLA-2 on cholangiocytes, normalization of 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: C max when administered 50 mg after 30, 60, 90 min - 3.8 mmol / L, 5.5 mmol / l and 3.7 mmol / l, respectively. C max is achieved in 1-3 hours.
The connection with proteins is high - up to 96-99%. Penetrates through the placental barrier. With the systematic administration of holudeksana-UDCA becomes the main bile acid in the 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.UDCA in bile.
Metabolised in the liver (clearance during primary passage through the liver) into taurine and glycine conjugates. The resulting conjugates are secreted into bile.About-50-70% of the total dose of the drug is excreted by bile. A small amount of unsweetened UDCA enters the thick / intestine; where it undergoes cleavage by bacteria: (dehydroxylation); the resulting lithocholic acid is partially absorbed from the colon, but sulfated in the liver and rapidly excreted as a sulfolithocholyl glycine, or sulfolitocholyltaurine conjugate.
INDICATIONS
- uncomplicated cholelithiasis (biliary sludge, dissolution of cholesterol gallstones in the gallbladder if they can not be removed by surgical or endoscopic methods, prevention of recurrence of stone formation after cholecystectomy);
- chronic active hepatitis;
- toxic (including medicinal) liver damage;
- alcoholic liver disease (ABP);
- non-alcoholic steatohepatitis;
- primary biliary cirrhosis of the liver;
- primary sclerosing cholangitis;
- cystic fibrosis;
- atresia of the intrahepatic biliary tract, congenital atresia of the bile duct;
- biliary dyskinesia;
- Biliary reflux-gastritis and reflux-esophagitis.
DOSING MODE
Choludexan is taken by mouth with a sufficient amount of water, with biliary reflux gastritis and reflux esophagitis - 1 time per day, before bedtime, with diffuse liver diseases - 2-3 times a day with food.
Chronic liver disease, cholelithiasis (cholesterol gallstones and biliary sludge) - continuously for a long time (from several months to several years) in a daily dose - from 10 mg / kg 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.
With biliary reflux gastritis and reflux esophagitis - 300 mg (1 capsule) per day, before bedtime. The course of treatment is from 10-14 days to 6 months, if necessary up to 2 years.
After cholecystectomy, for the prevention of recurrent cholelithiasis - 300 mg 2 times a day for several months.
Toxic, medicinal liver damage, ABP and atresia of the bile ducts - 10-15 mg / kg / day for 6-12 months or more.
Primary biliary cirrhosis - 10-15 mg / kg / day (if necessary - up to 20 mg / kg) from 6 months to several years.
Primary sclerosing cholangitis is 12-15 mg / kg / day, (up to 20 mg / kg) from 6 months to several years.
Non-alcoholic steatohepatitis is 13-15 mg / kg / day from 6 months to several years.
Cystic fibrosis - 20-30 mg / kg / day (up to 20 mg / kg) from 6 months to several years.
Children older than 3 years UDHK appoint individually, at a rate of 10-20 mg / kg / day.
SIDE EFFECT
Back pain, nausea, vomiting, diarrhea (may be dose-dependent), constipation, transient (transient) increase in hepatic transaminase activity, allergic reactions; rarely - calcification of gallstones, exacerbation of previously existing psoriasis, alopecia.
CONTRAINDICATIONS
- X-ray positive (high in calcium) gallstones;
- non-functioning gallbladder;
- a bile-gastric fistula;
- Acute cholecystitis;
- Acute cholangitis;
- cirrhosis of the liver in the stage of decompensation;
- acute infectious diseases of the gallbladder, bile ducts and intestines;
- marked hepatic and / or renal insufficiency;
- Obturation of the bile ducts;
- Empyema of the gallbladder;
- Children's age up to 3 years;
hypersensitivity to the drug.
With caution: although UDCA. has no age limitations in the use, with caution apply, Holudexan capsules in children aged 3 to 4 years, t. possible difficulty in swallowing capsules.
PREGNANCY AND LACTATION
Women of childbearing age during the period of drug use are advised to use non-hormonal contraceptives. The use of UDCA in pregnancy is possible only if the expected benefit for the mother exceeds the potential risk for the fetus (adequate strictly controlled studies of the use of UDCA in pregnant women have not been conducted). Data on the isolation of UDCA with breast milk are currently not available. If UDCA is necessary in the period of lactation, the question of stopping breastfeeding should be addressed
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe hepatic insufficiency.
APPLICATION FOR CHILDREN
Since it may be difficult to swallow the capsules, the drug should not be used in this dosage form in children under 3 years of age; in children from 3 to 4 years of age is used with caution.
SPECIAL INSTRUCTIONS
When taking the drug for the purpose of dissolution of gallstones, it is necessary to observe the following conditions: the stones must be cholesterol (X-ray negative), their size should not exceed 15-20 mm, the gallbladder should remain functional and should be filled with stones no more than half, the permeability of the cystic and of the common bile duct should be preserved. With prolonged (more than 1 month) taking the drug every 4 weeks in the first 3 months of treatment, then - every 3 months to conduct a biochemical blood test to determine the activity of hepatic transaminases. Control of the effectiveness of treatment should be carried out every 6 months according to ultrasound and radiographic examination of the biliary tract. After complete dissolution of the stones, it is recommended that the use of Choludexan be continued for at least 3 months in order to facilitate the dissolution of stone remains too small to detect them and to prevent the recurrence of stone formation.
If within 6 months after the initiation of therapy, partial dissolution of the stones did not occur, it is unlikely that the treatment will be effective.
Use in Pediatrics
Since it may be difficult to swallow the capsules, the drug should not be used in this dosage form in children under 3 years of age; in children from 3 to 4 years of age is used with caution.
Impact on the ability to drive vehicles and manage mechanisms
The drug does not adversely affect the ability to drive vehicles and / or other mechanisms.
OVERDOSE
Cases of overdose UDCA are not known.
DRUG INTERACTION
Antatsida containing aluminum and ion-exchange resins (colestyramine), reduce the absorption of the drug. Lipid-lowering drugs (especially clofibrate estrogens, neomycin or progestins increase
saturation of bile with cholesterol and can reduce the ability to dissolve cholesterol bile stones. Increases the effect of oral hypoglycemic drugs.
TERMS OF RELEASE FROM PHARMACY
On prescription.
TERMS AND CONDITIONS OF STORAGE
Store at a temperature of 15 to 25 В° C. Keep out of the reach of children. Shelf life is 3 years.
