Description
Pharmacological action
Pharmacodynamics
Hepatoprotective agent, has a choleretic effect. Reduces cholesterol synthesis in the liver, its absorption in the intestine and concentration in bile, increases the solubility of cholesterol in the biliary system, stimulates the formation and excretion of bile. Reduces the lithogenicity of bile, increases the content of bile acids in it, increases gastric and pancreatic secretion, enhances lipase activity, and has a hypoglycemic effect. Causes partial or complete dissolution of cholesterol stones when used internally, reduces the saturation of bile with cholesterol, which helps mobilize cholesterol from gallstones. It has an immunomodulatory effect, affects immunological reactions in the liver: reduces the expression of certain antigens on the hepatocyte membrane, affects the number of T-lymphocytes, the formation of ititerleukin-2, and reduces the number of eosinophils.
Pharmacokinetics
Ursodeoxycholic acid (UDCA) is absorbed in the small intestine by passive diffusion (about 90%), and in the ileum by active transport. After oral administration in a single dose (500 mg), the maximum concentration in blood serum (Cmax) after 30, 60, 90 min is 3.8, 5.5, 3.7 mmol / L, respectively. Communication with plasma proteins is high – up to 96-99%. Penetrates through the placental barrier. With systematic administration, ursodeoxycholic acid becomes the main serum bile acid (48% of the total bile acid content). The therapeutic effect of the drug depends on the concentration of UDCA in bile.
Metabolized in the liver (clearance during the initial passage through the liver) to taurine and glycine conjugates. The resulting conjugates are secreted into the bile. About 50-70% of the total dose is excreted through the intestines. A small amount of non-absorbable Ursodeoxycholic acid enters the large intestine, where it is digested by bacteria (7-dehydroxylation), the resulting lithocholic acid is partially absorbed from the colon, but sulfates in the liver and is rapidly excreted as sulfolithocholylglycimene or sulfolithocholyltauric acid.
Indications
Dissolution of small and medium cholesterol stones with a functioning gall bladder, biliary reflux gastritis, primary biliary cirrhosis with no signs of decompensation (symptomatic treatment).
Chronic hepatitis of various origins, primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis), non-alcoholic steatohepatitis, alcoholic liver disease, biliary dyskinesia.
Contraindications
X-ray positive (high in calcium) gallstones
Mefumciating gallbladder
Acute inflammatory diseases of the gallbladder, bile ducts and intestines
Liver cirrhosis in the decompensation stage of liver disease, expressive liver function
Adults and children weighing up to 34 kg
Children under 3 years of age for this dosage form.
Caution
Use with caution in the following conditions: with gallstone disease, with cholestatic liver disease (see section “Special Instructions”).
Use during pregnancy and lactation
The drug is contraindicated during pregnancy and breastfeeding.
Special instructions
Urosodez ® should be taken under medical supervision.
During the first 3 months of treatment, the functional parameters of the liver (transaminases, alkaline phosphatase and gamma-glutamyl transpeptidase) in the blood serum should be monitored every 4 weeks, and then every 3 months.
Monitoring of these parameters reveals impaired liver function in the early stages. This also applies to patients in the later stages of primary biliary cirrhosis. In addition, this way you can quickly determine whether a patient with primary biliary cirrhosis responds to treatment.
When used to dissolve cholesterol gallstones:
In order to assess progress in treatment and to detect signs of calcification of stones in a timely manner, the gall bladder should be visualized (oral cholecystography) with examination of the blackouts in the “standing” and “lying on the back” positions (ultrasound examination) 6-10 months after the start of the study. If the gallbladder cannot be visualized on x-rays or in cases of calcification of stones, weak contractility of the gallbladder or frequent bouts of colic, the drug Ursodez ® should not be used.
In the treatment of patients in the late stages of primary biliary cirrhosis: Very rarely, there have been cases of decompensation of liver cirrhosis.
After discontinuation of therapy, a regression of manifestations of decompensation was noted.
Long-term therapy with high doses of ursodeoxycholic acid (28-30 mg / kg / day) can lead to the development of serious side effects in patients with primary sclerosing cholangitis.
In patients with diarrhea, the dosage of the drug should be reduced. With persistent diarrhea, treatment should be discontinued.
Influence on the ability to drive vehicles and control mechanisms
Influence on the ability to drive vehicles, mechanisms not identified.
Composition
Active ingredient: ursodeoxycholic acid-250 mg
excipients: pregelatinized starch (starch, silica, 1500 mg) – 73.0 – 73.0 aerosil) – 5.0 mg, magnesium stearate – 2.0 mg
capsule shell: body and cap: titanium dioxide – 2.1118%, gelatin – up to 100%
Dosage and Administration
Inside.
Dissolution of cholesterol gallstones
The recommended (approximate) dose is 10 mg of ursodeoxycholic acid per 1 kg of body weight per day. The drug must be taken daily in the evening, before bedtime (capsules do not chew), washed down with a small amount of liquid.
It usually takes 6-24 months to dissolve gallstones. If after 12 months of treatment the size of the stones does not decrease, then treatment should be discontinued.
Treatment efficacy should be evaluated every 6 months with ultrasound or radiography. During the interim examination, it should be assessed whether calcification of stones has occurred over the past period. In case of calcification of stones, treatment should be discontinued.
To prevent re-cholelithiasis, it is recommended to take the drug for several months after the stones dissolve.
Treatment of biliary reflux gastritis
1 capsule (250 mg) of Ursodez ® daily in the evening before bedtime with a little water.
The course of treatment is 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 ranges from 1 to 3 capsules (500 mg) or 2 to 6 capsules (250 mg) (approximately 10 to 15 mg of ursodeoxycholic acid per 1 kg of body weight) 2 – 3 doses, the first 3 months of treatment. After improving the functional parameters of the liver, the daily dose can be applied once in the evening. The duration of treatment is not limited. In rare cases, clinical symptoms may worsen at the beginning of treatment (itching becomes more frequent). In this case, the daily dose should be reduced (to 250 mg), and then gradually increase it (increasing the daily dose weekly) until the recommended dosage regimen is reached.
For chronic hepatitis of various origins, non-alcoholic steatohepatitis and alcoholic liver disease
The average daily dose is from 10 to 15 mg of ursodeoxycholic acid per 1 kg of body weight in 2-3 doses. The duration of therapy is 6-12 months or more.
With primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis)
With primary sclerosing cholangitis: 12-15 mg / ct / day (up to 20 mg / kg) body weight per day in 2-3 doses. Duration of use – from 6 months to several years. With cystic fibrosis (cystic fibrosis): 20-30 mg / kg per day in 2 to 3 doses. Duration of use – from 6 months to several years.
For biliary dyskinesia
The average daily dose is 10 mg of ursodeoxycholic acid per 1 kg of body weight in 2 divided doses for 2 weeks to 2 months. If necessary, the treatment should be repeated.
Dosage regimen is determined by the doctor.
table.
Calculation of the daily number of capsules depending on the patient ² ¢s body weight and recommended dose of the drug pa 1 kg body weight
Body weight, kg
10 mg / kg / day
12 mg / kg / day
15 mg / kg / day
20 mg / kg / day
30 mg / kg / day
34-35 1 caps. 250 mg 2 caps. 250 mg or 1 capsule. 500 mg 2 caps. 250 mg or 1 capsule. 500 mg 3 caps. 250 mg 4 caps. 250 mg or 2 caps. 500 mg
36-40 2 caps. 250 mg or 1 capsule. 500 mg 2 caps. 250 mg or 1 capsule. 500 mg 2 caps. 250 mg or 1 capsule. 500 mg 3 caps. 250 mg 5 caps. 250 mg
41-45 2 caps. 250 mg or 1 capsule. 500 mg 2 caps. 250 mg or 1 capsule. 500 mg 3 caps. 250 mg 4 caps. 250 mg or 2 caps. 500 mg 5 caps. 250 mg
45-50 2 caps. 250 mg or 1 capsule. 500 mg 2 caps. 250 mg or 1 capsule. 500 mg 3 caps. 250 mg 4 caps. 250 mg or 2 caps. 500 mg 6 caps. 250 mg or 3 caps. 500 mg
51-55 2 caps. 250 mg or 1 capsule. 500 mg 3 caps. 250 mg 3 caps. 250 mg 1 capsule. 250 mg or 2 caps. 500 mg 7 caps. 250 mg
86 – 90 4 caps. 250 mg or 2 caps. 500 mg 4 caps. 250 mg or 2 caps. 500 mg 5 caps. 250 mg 7 caps. 250 mg 10 caps. 250 mg or 5 caps. 500 mg
91 -95 4 caps. 250 mg or 2 caps. 500 mg 5 caps. 250 mg 6 caps. 250 mg or 3 caps. 500 mg 8 caps. 250 mg or 4 caps. 500 mg 11 caps. 250 mg
96-100 4 caps. 250 mg or 2 caps. 500 mg 5 caps. 250 mg 6 caps. 250 mg or 3 caps. 500 mg 8 caps. 250 mg or 4 caps. 500 mg 12 caps. 250 mg or 5 caps. 500 mg
101-105 4 caps. 250 mg or 2 caps. 500 mg 5 caps. 250 mg 6 caps. 250 mg or 3 caps. 500 mg 8 caps. 250 mg or 4 caps. 500 mg 13 caps. 250 mg
105-110 4 caps. 250 mg or 2 caps. 500 mg 5 caps. 250 mg 7 caps. 250 mg 9 caps. 250 mg 13 caps. 250 mg
For children from 3 years of age
Individually (at the rate of 10-20 mg / kg per day).
Side effects
Diarrhea, nausea, pain in the epigastric region and right hypochondrium, calcification of gallstones, increased activity of hepatic transaminases, allergic reactions.
In the treatment of primary biliary cirrhosis, transient decompensation of cirrhosis of the liver may occur, which disappears after discontinuation of the drug.
Drug Interactions
Colestyramine, colestipol and antacids containing aluminum hydroxide or smectite (aluminum oxide) reduce the absorption of ursodeoxycholic acid in the intestine and thus reduce its absorption and effectiveness. If the use of drugs containing at least one of these substances is nevertheless necessary, they must be taken at least 2 hours before taking the drug Ursodez ®.
Ursodeoxycholic acid may enhance absorption of cyclosporine from the intestines. Therefore, in patients taking cyclosporine, the doctor should check the concentration of cyclosporin in the blood and adjust the dose of cyclosporine if necessary.
In some cases, Ursodez ® may decrease the absorption of ciprofloxacin.
Hypolipidemic drugs (especially clofibrate), estrogens, neomycin, or progestins increase bile saturation with cholesterol and may decrease the ability to dissolve cholesterol bile calculi.
Overdose
There have been no cases of overdose. In case of an overdose, symptomatic treatment is performed.
Storage conditions
In a dry, dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.
Deystvuyuschee substances
ursodeoxycholic acid
Terms and conditions
prescription
dosage form
capsules
