Description
Release form
Tablets, film-coated white or almost white, oblong, biconvex, with a notch on one side and a deep separating risk on the other side on the break – white or almost white.
Pharmacological action
Hepatoprotective drug. It also has choleretic, cholelitholytic, hypolipidemic, hypocholesterolemic and immunomodulatory effects. With its high polar properties, ursodeoxycholic acid (UDCA) integrates into the membrane of the hepatocyte, cholangiocyte and gastrointestinal epithelial cell, stabilizes its structure and protects the cell from the damaging effects of toxic bile salts, thus reducing their cytotoxic effect. It forms non-toxic mixed micelles with lipophilic (toxic) bile acids, which reduces the ability of gastric reflux to damage cell membranes with cholestatic liver diseases, biliary reflux gastritis and reflux esophagitis.
In case of cholestasis, UDCA activates a Ca2-dependent alpha protease and stimulates exocytosis, reduces the concentration of toxic bile acids (chenodeoxycholic, lithocholic, deoxycholic, etc.), whose concentrations in patients with chronic liver diseases are increased. By reducing their concentration and stimulating bicarbonate-rich choleresis, UDCA effectively helps resolve intrahepatic cholestasis. Competitively reduces the absorption of lipophilic bile acids in the intestine, increases their fractional circulation during enterohepatic circulation, induces choleresis, stimulates the passage of bile and the elimination of toxic bile acids through the intestines.
Reduces the saturation of bile with cholesterol by inhibiting its absorption in the intestine, suppressing synthesis in the liver and lowering secretion into bile, which contributes to the gradual decomposition of cholesterol gallstones, which is achieved mainly due to the dispersion of cholesterol and the formation of liquid crystals, reduces the lithogenic index of bile, increases the concentration of bile in it acids. The result is the dissolution of cholesterol gallstones and the prevention of the formation of new calculi.
Causes increased gastric and pancreatic secretion, enhances lipase activity, has a hypoglycemic effect.
The immunomodulatory effect of UDCA is due to inhibition of the expression of histocompatibility antigens – HLA-1 – on hepatocyte membranes and HLA-2 – on cholangiocytes, normalization of the natural killer activity of lymphocytes, formation of interleukin-2, a decrease in the number of eosinophils, first immuno-urine counts – IgM regulation of apoptosis of hepatocytes and gastrointestinal epithelial cells. Delays the progression of fibrosis.
Indications
– uncomplicated gallstone disease: biliary sludge dissolving cholesterol gallstones with a functioning gallbladder prevention of recurrence of stone formation after cholecystectomy
– chronic hepatitis of various origins (including toxic, drug-induced liver disease) .h. primary biliary cirrhosis (in the absence of signs of decompensation), primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis)
– non-alcoholic fatty liver disease, including non-alcoholic steatohepatitis
– alcoholic liver disease
– chronic viral hepatitis
– biliary dyskinesia
– biliary reflux gastritis and reflux esophagitis.
Contraindications
– hypersensitivity to the active and auxiliary components of the drug
– x-ray positive (high calcium) gallstones
– nonfunctioning gallbladder
– acute inflammatory diseases of the gallbladder, bile ducts and intestines srclpcrpdcrpcrp pronounced renal dysfunction
– severe hepatic dysfunction
– severe pancreatic dysfunction.
Ursodeoxycholic acid has no age restrictions for use, however, in children under the age of 3 years, it is not recommended to use the drug in this dosage form.
Use during pregnancy and lactation
The use of ursodeoxycholic acid during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus or newborn (there are no adequate strictly controlled studies on the use of ursodeoxycholic acid in pregnant women).
Women of reproductive age should take the drug Ursosan while using reliable contraceptives. Before starting treatment, pregnancy should be excluded.
There are no data on the release of ursodeoxycholic acid in breast milk. If necessary, the use of ursodeoxycholic acid during lactation should stop breastfeeding.
Special instructions
The use of the drug to dissolve gallstones is possible under the following conditions: the stones must be cholesterol (X-ray negative), their size should be no more than 15-20 mm, a functioning gallbladder with preserved patency of the cystic and common bile duct, filled with bile stones no more than half.
With prolonged use of the drug to dissolve gallstones every 4 weeks in the first 3 months of treatment, then every 3 months a biochemical blood test should be performed to determine the activity of hepatic transaminases. Monitoring the effectiveness of treatment should be carried out every 6 months according to ultrasound of the gallbladder, biliary tract.
After complete dissolution of the stones, it is recommended to continue using the drug for 3 months in order to help dissolve the remnants of stones that are too small to detect, and to prevent the recurrence of stone formation.
Impact on the ability to drive vehicles and mechanisms
The use of the drug Ursosan does not affect the performance of potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions (including the ability to drive vehicles, work with moving mechanisms).
Composition
1 tab. – ursodeoxycholic acid 500 mg
Excipients:
corn starch – 94.5 mg,
pregelatinized corn starch – 48 mg,
sodium carboxymethyl starch (type A) – 13 mg,
silicon colloidal dioxide – 15 mg,
magnesium stearate – 14.5 mg.
Dosage and administration
Take orally, during or after a meal, without chewing, with plenty of water.
To ensure the recommended dose, the tablet should be divided in half, breaking at risk. Segments broken wrong should not be used. When you hold a segment in the oral cavity, a bitter taste is felt.
To dissolve cholesterol gallstones, the average daily dose is 10 mg / kg (up to 12-15 mg / kg). The daily dose is taken once at night. The course of treatment is 6-12 months or more until the stones completely dissolve. If the stones in the gallbladder do not decrease in size after 12 months of treatment, the drug should be discontinued.
To prevent re-formation of stones, it is recommended to use the drug for several months after the stones dissolve.
To prevent re-cholelithiasis after cholecystectomy, 250 mg (1 caps. or 1/2 tab.) is prescribed 2 times / day for several months.
For chronic hepatitis of various origins (including toxic, medicinal), chronic viral hepatitis, non-alcoholic fatty liver disease, including non-alcoholic steatohepatitis, alcoholic liver disease, the average daily dose is 10-15 mg / kg in 2-3 doses. The duration of therapy is 6-12 months or more.
With cholestatic diseases of the liver of various origins, including primary biliary cirrhosis (in the absence of signs of decompensation), primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis), the average daily dose is 12-15 mg / kg, if necessary, 20-30 mg / kg. During the first 3 months of treatment, the daily dose should be divided into 2-3 doses. In case of improvement of blood biochemical parameters, the daily dose of the drug is taken once at night. The duration of therapy is from 6 months to several years.
With biliary dyskinesia, the average daily dose is 10 mg / kg in 2 divided doses for 2 weeks to 2 months. If necessary, the treatment is recommended to be repeated.
With biliary reflux gastritis and reflux esophagitis, the average daily dose is 250 mg (1 caps. or 1/2 tab.) 1 time per night. The course of treatment is from 2 weeks to 6 months, if necessary – up to 2 years.
Calculation of the daily number of capsules and tablets depending on the patient s body weight and the recommended dose of the drug per 1 kg of body weight, mg / kg / day
Body weight, kg 10 mg / kg / day 12 mg / kg / day 15 mg / kg / day 20 mg / kg / day 30 mg / kg / day
1 2 3 4 5 6
19-25 1/2 tab.
or
1 caps. 1/2 tab.
or
1 caps. 1 tab
or
2 caps. 1 tab
or
2 caps. 1 and 1/2 tab.
or
3 caps.
26-30 1/2 tab.
or
1 caps. 1/2 tab.
or
1 caps. 1 tab
or
2 caps. 1 tab
or
2 caps. 1 and 1/2 tab.
or
3 caps.
31-35 1/2 tab.
or
1 caps. 1 tab
or
2 caps. 1 tab
or
2 caps. 1 and 1/2 tab.
or
3 caps. 2 tab.
or
4 caps.
36-40 1 tab.
or
2 caps. 1 tab
or
2 caps. 1 tab
or
2 caps. 1 and 1/2 tab.
or
3 caps. 2 and 1/2 tab.
or
5 caps.
41-45 1 tab.
or
2 caps. 1 tab
or
2 caps. 1 and 1/2 tab.
or
3 caps. 2 tab.
or
4 caps. 2 and 1/2 tab.
or
5 caps.
45-50 1 tab.
or
2 caps. 1 tab
or
2 caps. 1 and 1/2 tab.
or
3 caps. 2 tab.
or
4 caps. 3 tab.
or
6 caps.
51-55 1 tab.
or
2 caps. 1 and 1/2 tab.
or
3 caps. 1 and 1/2 tab.
or
3 caps. 2 tab.
or
4 caps. 3 and 1/2 tab.
or
7 caps.
56-60 1 tab.
or
2 caps. 1 and 1/2 tab.
or
3 caps. 2 tab.
or
4 caps. 2 and 1/2 tab.
or
5 caps. 3 and 1/2 tab.
or
7 caps.
61-65 1 and 1/2 tab.
or
3 caps. 1 and 1/2 tab.
or
3 caps. 2 tab.
or
4 caps. 2 and 1/2 tab.
or
5 caps. 4 tab.
or
8 caps.
66-70 1 and 1/2 tab.
or
3 caps. 1 and 1/2 tab.
or
3 caps. 2 tab.
or
4 caps. 3 tab.
or
6 caps. 4 tab.
or
8 caps.
71-75 1 and 1/2 tab.
or
3 caps. 2 tab.
or
4 caps. 2 and 1/2 tab.
or
5 caps. 3 tab.
or
6 caps. 4 and 1/2 tab.
or
9 caps.
76-80 1 and 1/2 tab.
or
3 caps. 2 tab.
or
4 caps. 2 and 1/2 tab.
or
5 caps. 3 tab.
or
6 caps. 5 tab.
or
10 caps.
81-85 1 and 1/2 tab.
or
3 caps. 2 tab.
or
4 caps. 2 and 1/2 tab.
or
5 caps. 3 and 1/2 tab.
or
7 caps. 5 tab.
or
10 caps.
86-90 2 tab.
or
4 caps. 2 tab.
or
4 caps. 2 and 1/2 tab.
or
5 caps. 3 and 1/2 tab.
or
7 caps. 5 and 1/2 tab.
or
11 caps.
91-95 2 tab.
or
4 caps. 2 and 1/2 tab.
or
5 caps. 3 tab.
or
6 caps. 4 tab.
or
8 caps. 5 and 1/2 tab.
or
11 caps.
96-100 2 tab.
or
4 caps. 2 and 1/2 tab.
or
5 caps. 3 tab.
or
6 caps. 4 tab.
or
8 caps. 6 tab.
or
12 caps.
101-105 2 tab.
or
4 caps. 2 and 1/2 tab.
or
5 caps. 3 tab.
or
6 caps. 4 tab.
or
8 caps. 6 and 1/2 tab.
or
13 caps.
105-110 2 tab.
or
4 caps. 2 and 1/2 tab.
or
5 caps. 3 and 1/2 tab.
or
7 caps. 4 and 1/2 tab.
or
9 caps. 6 and 1/2 tab.
or
13 caps.
Side effects
Determination of the frequency of side effects (number of cases / number of cases): very often (? 1/10) often (? 1/100 to <1/10) infrequently (? 1/1000 to From the digestive system: In clinical trials, diarrhea or pasty stools were often observed during treatment with ursodeoxycholic acid.In the treatment of primary biliary cirrhosis, severe pain in the upper abdomen was very rarely observed. From the liver and biliary tract: during treatment with ursodeoxycholic acid in very rare cases, calcification of gallstones was observed. In the treatment of primary biliary cirrhosis in the late stages, in very rare cases, decompensation of cirrhosis of the liver was observed, which regressed after discontinuation of treatment. From the skin and subcutaneous tissues: in very rare cases, urticaria may be observed. Drug Interactions The drug should not be used simultaneously with antacids containing aluminum, ion-exchange resins (colestyramine, colestipol), since these drugs can reduce the absorption of ursodeoxycholic acid. If necessary, these drugs should be taken 2 hours before or 2 hours after receiving UDCA. Some drugs, such as estrogens, progestogens (oral contraceptives), neomycin, clofibrate, can increase cholelithiasis, thereby providing the opposite effect of the ability of ursodeoxycholic acid to dissolve cholesterol bile calculi. Ursodeoxycholic acid can increase the absorption of cyclosporin from the intestine, which requires monitoring the concentration of cyclosporin in the blood plasma, and if necessary, correcting its dosage regimen. In some cases, ursodeoxycholic acid may decrease the absorption of ciprofloxacin. Overdose Symptoms: in case of overdose, diarrhea may occur. Other symptoms of an overdose are unlikely, since the resorption of ursodeoxycholic acid worsens with increasing dose, which leads to increased excretion of it with feces. Treatment: With established long-term diarrhea, drug therapy should be discontinued. Treatment is symptomatic. Storage Conditions Tablets should be stored in a dark place and at a temperature of 15 ° to 25 ° C. Expiration 3 years. Active ingredient Ursodeoxycholic acid Terms leave through pharmacies In retseptu lekarstvennaja form tablets
