Урсодез® капс 250 mg No. 50/100

General characteristics. Structure:

Active agent: ursodezoksikholevy acid – 250 mg;
excipients: starch prezhelatinizirovanny (starch 1500) – 73,0 mg, silicon dioxide colloid (aerosil) – 5,0 mg, magnesium stearate – 2,0 mg
capsule cover: titanium dioxide, gelatin.

Description. Solid, white, opaque gelatin capsules.
The capsule size – No. 0.
Contents of capsules – powder of white or almost white color.

Pharmacological properties:

Pharmacodynamics. Hepatoprotective means, has cholagogue effect. Reduces synthesis of cholesterol in a liver, its absorption in intestines and concentration in bile, increases solubility of cholesterol in bile-excreting system, stimulates education and biliation. Reduces a bile litogennost, increases in it the content of bile acids; causes strengthening of gastric and pancreatic secretion, increases activity of a lipase, has hypoglycemic effect. Causes partial or full dissolution of cholesteric stones at enteral use, reduces a bile saturation cholesterol that promotes mobilization of cholesterol from gallstones. Has immunomodulatory effect, influences immunological reactions in a liver: reduces an expression of some antigens on a membrane of hepatocytes, influences quantity of T lymphocytes, education interleykina-2, reduces quantity of eosinophils.

Pharmacokinetics. Ursodezoksikholevy acid (UDHK) is absorbed in a small bowel due to passive diffusion (about 90%), and in an ileal gut by means of active transport. After intake in a single dose (500 mg) the maximum concentration in blood serum (Cmax) in 30, 60, 90 min. makes 3.8, 5.5, 3.7 mmol/l respectively. Communication with proteins of plasma - high - to 96-99%. Gets through a placental barrier. At systematic reception ursodezoksikholevy acid becomes the main bile acid of blood serum (48% of the general contents of bile acids). The therapeutic effect of drug depends on concentration of UDHK in bile. It is metabolized in a liver (clearance at "primary passing" through a liver) in taurinovy and glycine conjugates. The formed conjugates cosecrete in bile. About 50-70% of the general dose are removed through intestines. The insignificant amount of not soaked up ursodezoksikholevy acid comes to a large intestine where is exposed to splitting by bacteria (7 dehydroxylation); the formed lithocholic acid partially is soaked up from a large intestine, but sulphated in a liver and quickly removed in the form of a sulfolitokholilglitsinovy or sulfolitokholiltaurinovy conjugate.

Indications to use:

Dissolution of cholesteric stones of a gall bladder, biliary reflux gastritis, primary biliary cirrhosis in the absence of signs of a decompensation (symptomatic treatment). Chronic hepatitises of various genesis, primary sclerosing cholangitis, cystous fibrosis (mucoviscidosis), not alcoholic steatogepatit, an alcoholic liver disease, dyskinesia of biliary tract.

Route of administration and doses:

Inside.
Dissolution of cholesteric gallstones
The recommended (approximate) dose makes 10 mg of ursodezoksikholevy acid on 1 kg of body weight a day. Drug needs to be accepted daily in the evening, before going to bed (the capsule is not chewed), washing down with a small amount of liquid. Duration of treatment is 6-12 months. For prevention of a repeated cholelithiasis administration of drug within several months after dissolution of stones is recommended.
Treatment biliary reflux gastritis
1 capsule of the drug Ursodez® daily in the evening before going to bed, washing down with a small amount of water. A 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 body weight and makes from 2 to 6 capsules (from about 10 to 15 mg of ursodezoksikholevy acid on 1 kg of body weight) in 2-3 receptions.
At chronic hepatitises of various genesis, not alcoholic steatogepatit and an alcoholic liver disease
The average daily dose makes from 10 to 15 mg of ursodezoksikholevy acid on 1 kg of body weight in 2-3 receptions. Duration of therapy makes 6-12 months and more.
At primary sclerosing cholangitis, cystous fibrosis (mucoviscidosis)
The average daily dose makes from 12 to 15 mg of ursodezoksikholevy acid on 1 kg of body weight; if necessary the average daily dose can be increased to 20-30 mg by 1 kg of body weight in 2-3 receptions. Duration of therapy makes from 6 months to several years.
At dyskinesia of biliary tract
The average daily dose makes 10 mg of ursodezoksikholevy acid on 1 kg of body weight in 2 receptions during from 2 weeks to 2 months. If necessary the course of treatment needs to be repeated.

Calculation of daily number of capsules depending on the body weight of the patient and the recommended drug dose on 1 kg of body weight.

Features of use:

At cholelithiasis control of efficiency of treatment is exercised each 6 months by carrying out radiological and ultrasound examination of biliary tract for the purpose of prevention of a recurrence of a cholelithiasis. At cholestatic diseases of a liver it is necessary to define periodically activity of transaminases, an alkaline phosphatase and gamma глютамилтранспептидазы in blood serum.

Side effects:

Diarrhea, nausea, pain in epigastric area and the right hypochondrium, calcination of gallstones, increase in activity of "hepatic" transaminases, allergic reactions. At treatment of primary biliary cirrhosis the passing decompensation of cirrhosis which disappears after drug withdrawal can be observed.

Interaction with other medicines:

Colestyraminum, колестипол and the antacids containing aluminum hydroxide or smectite (aluminum oxide), reduce absorption of ursodezoksikholevy acid in intestines and thus reduce its absorption and efficiency. If use of the drugs containing at least one of these substances nevertheless is necessary, it is necessary to accept them a minimum in 2 hours prior to administration of drug of Ursodez®. Ursodezoksikholevy acid can strengthen absorption of cyclosporine from intestines. Therefore at the patients accepting cyclosporine, the doctor has to check concentration of cyclosporine in blood and correct a cyclosporine dose in case of need. In some cases Ursodez® can reduce ciprofloxacin absorption. Hypolipidemic medicines (especially Clofibratum), are oestrogenic, Neomycinum or progestins increase bile saturation by cholesterol and can reduce ability to dissolve cholesteric bilious concrements.

Contraindications:

- Rentgenpolozhitelnye (with the high content of calcium) gallstones;
- Nonfunctioning gall bladder;
- Acute inflammatory diseases of a gall bladder, bilious channels and intestines;
- Cirrhosis in a decompensation stage;
- The expressed abnormal liver functions, kidneys, a pancreas;
- Hypersensitivity to drug components;
- Adults and children with body weight to 34 kg.

Overdose:

Cases of overdose are not revealed. In case of overdose carry out a symptomatic treatment.

Storage conditions:

Period of validity: 5 years. Not to use after the period of validity specified on packaging. In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Capsules of 250 mg. On 10 capsules in a blister strip packaging. On 10, 50, 100 capsules in bank of light-protective glass or bank polymeric, or in a bottle polymeric. Each can or a bottle, 1, 5 or 10 blister strip packagings together with the application instruction are placed in a pack from a cardboard.