Ursodeoxycholic acid is absorbed in the small intestine due to passive diffusion (approximately 90%) and in the ileum by an active transport. After oral administration in a single dose (500 mg), the maximum serum concentration (Cmax) after 30, 60, 90 minutes is 3.8, 5.5, 3.7 mmol / l, respectively. Connection with the plasma protein -high – up to 96-99%. It penetrates through the placental barrier. At regular ursodeoxycholic acid it becomes the primary bile acid serum (48% of total bile acids). The therapeutic effect of the drug is dependent on the concentration of in bile.
It is metabolized in the liver (clearance at “primary pass” through the liver) in the taurine and glycine conjugates. The resulting conjugates are secreted into bile. Approximately 50-70% of testosterone injections the dose is excreted through the intestines. A small number of nevsosavsheysya ursodeoxycholic acid enters the large intestine, where bacteria undergoes cleavage ; lithocholic acid formed partially absorbed from the colon, but sulfated in the liver and rapidly excreted in the form sulfolitoholilglitsimovogo or sulfolitoholiltaurinovogo conjugate.
Indications for use
Dissolution of small and medium-sized stones with cholesterol functioning gallbladder, biliary reflux gastritis, primary biliary cirrhosis in the absence of signs of decompensation (symptomatic treatment).
Chronic hepatitis of various origins, primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis), iealkogolny steatohepatitis, alcoholic liver disease, biliary dyskinesia.
- Rentgenpolozhitelnye (high in calcium) gallstones;
- Mefumktsiomiruyuschy gall bladder;
- Acute inflammatory diseases of the gallbladder, bile ducts and intestines;
- Cirrhosis decompensated;
- Expressed human liver, kidney, pancreas;
- Hypersensitivity to the drug;
- Adults and children weighing up to 34 kg;
- Children up to age 3 years, for a given dosage form.
Use with caution in the following conditions: in cholelithiasis, in cholestatic liver diseases (see “Special Instructions” section.).
Application of pregnancy and during breastfeeding
The drug is contraindicated during pregnancy and breastfeeding.
Dosing and Administration
Dissolving cholesterol gallstones
Recommended (approximate) the dose is 10 mg testosterone injections of ursodeoxycholic acid per 1 kg of body weight per day. The drug must be taken daily in the evening, before going to bed (not chew the capsule), washed down with a small amount of liquid.
Usually it requires 6-24 months to dissolve gallstones. If, after 12 months of treatment, the size of the stones is not reduced, the treatment should be discontinued.
The effectiveness of treatment should be assessed every 6 months with ultrasound or radiography. During the intermediate surveys should be to assess whether the calcification of the stones in the intervening period has not occurred. In the case of calcification of stones, treatment should be discontinued.
For the prevention of cholelithiasis re-recommended the drug for several months after the dissolution of stones.
Treatment of biliary reflux gastritis
1 capsule (250 mg) of the every day in the evening before going to bed, with a little water.
The course of treatment 10-14 days to 6 months, if necessary – up to 2 years.
Symptomatic treatment of primary biliary cirrhosis
daily dose depends on the body weight and from 1 to 3 capsules (500 mg) or 2 to 6 capsules (250 mg) (from about 10 to 15 mg of ursodeoxycholic acid per 1 kg of body weight) 2 – 3 receiving the first 3 months of treatment. After the improvement of liver function parameters, the daily dose once in the evening can be used. The duration of treatment is not limited. In rare cases, early treatment can worsen the clinical symptoms (itching more frequent). In this case, to reduce the daily dose (250 mg), and then gradually increase it (by increasing the daily dose weekly) until until it reaches the recommended dosage regimen.
In chronic hepatitis of various genesis, nonalcoholic steatohepatitis and alcoholic liver disease
average daily dose is 10 to 15 mg of ursodeoxycholic acid per 1 kg of body weight in 2-3 divided doses. The duration of therapy is 6-12 months or more.
In primary sclerosing cholangitis, cystic fibrosis (mucoviscidosis)
in primary sclerosing cholangitis: 12-15 mg / rt / day (20 mg / kg) of body weight per day in 2-3 divided doses. Duration of treatment – from 6 months to several years. In cystic fibrosis (mucoviscidosis): 20-30 mg / kg per day in 3 divided doses 2. Duration of treatment – from 6 months to several years.
When biliary dyskinesia
average daily dose is 10 mg of ursodeoxycholic acid per 1 kg of body weight in 2 hours for 2 weeks to 2 months. If necessary, treatment must be repeated.
Dosage is determined by the doctor.
Diarrhea, nausea, pain in the testosterone injections epigastric and right upper quadrant, the calcination gallstones, increased activity of “liver” enzymes, allergic reactions.
In the treatment of primary biliary cirrhosis may be a transient decompensation of cirrhosis, which disappears after discontinuation of the drug.
No cases of overdose have been identified. In case of overdose symptomatic treatment.
Interaction with other drugs
Cholestyramine, colestipol, antacids that contain aluminum hydroxide or smectite (aluminum oxide), reduce the absorption of UDCA in the intestine and thereby reduce its absorption and efficacy. If the use of preparations containing at least one of these substances, yet necessary, they should be taken at least 2 hours before receiving the testosterone injections .
Ursodeoxycholic acid can enhance the absorption of cyclosporin from the gut. Therefore, in patients receiving cyclosporin, the physician must check the concentration of cyclosporine in the blood and to adjust the dose of cyclosporin, if necessary.
In some cases may reduce the absorption of ciprofloxacin.
Lipid-lowering drugs (particularly clofibrate), estrogens, neomycin or progestins increase the saturation of bile with cholesterol and may reduce the ability to dissolve cholesterol gallstones.