Ursoliv capsules 250 mg 100 pcs
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Active ingredients
Ursodeoxycholic acid
Composition
1 caps Ursodeoxycholic acid 250 mg. Excipients: lactulose - 300 mg, low molecular weight povidone K17 - 7.
Pharmacological effect
The drug has hepatoprotective, choleretic, cholelitholytic, hypolipidemic, hypocholesterolemic and some immunomodulatory effects. In vitro studies have shown that ursodeoxycholic acid (UDCA) has a direct protective effect on liver cells and reduces the hepatotoxicity of hydrophobic bile salts. The main effects of UDCA on cholesterol metabolism include: a decrease in cholesterol secretion, a decrease in its intestinal absorption, and the stimulation of cholesterol from cholesterol stones in bile. UDCA, inhibiting GMC-CoA reductase, also has a moderate inhibitory effect on cholesterol synthesis in the liver, increases the solubility of cholesterol in the biliary system. Causes the partial or complete dissolution of cholesterol gallstones during enteral use, reduces the saturation of bile with cholesterol. Stimulates the formation and secretion of bile, accelerates the excretion of toxic bile acids through the intestine. When taken orally, the proportion of UDCA in the total pool of bile acids increases significantly. UDCA competes with other bile acids in the process of absorption in the small intestine, as well as penetration of the hepatocyte through the membrane, which leads to a decrease in the absorption of toxic bile acids in the intestine and their entry into the liver, preventing their cytopathogenic action. It reduces the lithogenicity of bile, increases the concentration of bile acids in it, causes an increase in gastric and pancreatic secretion, enhances the activity of lipase, and has a hypoglycemic effect. It has an effect on immunological reactions, reducing the pathological expression of antigens of the main histocompatibility complex HLA І on hepatocytes and HLA II on cholangiocytes, inhibits the production of interleukin-2, reduces the number of eosinophils.
Pharmacokinetics
Absorption: UDCA is absorbed in the small intestine (about 90%), while Cmax in the blood plasma when the drug is taken orally at a dose of 250 mg is about 3.3 μg / ml, Tmax - about 2 hours. Distribution: Binding to plasma proteins of unconjugated UDCA in healthy people is at least 70%.It penetrates the placental barrier. When systematically taken in doses of 13-15 mg / kg / day, UDCA becomes the main bile acid in serum and makes up from 30 to 50% of the total bile acid in the blood. The therapeutic effect of the drug depends on the concentration of UDCA in the bile. Metabolism and excretion: Metabolized in the liver to become tauric and glycine conjugates that are secreted into bile. About 50-70% of the ingested dose of the drug is excreted in the bile. Removal with urine does not exceed 1%. A small amount of non-sucked after oral administration of UDCA enters the colon, where it is broken down by bacteria (7-dehydroxylation); The formed lithocholic acid is partially absorbed from the colon, sulphated in the liver and rapidly excreted in the form of a sulfolithocholyl glycine or sulfolithocholyl taurine conjugate.
Indications
- primary biliary cirrhosis in the absence of signs of decompensation (symptomatic therapy) - dissolution of small and medium cholesterol stones with a functioning gall bladder - biliary reflux-gastritis - chronic hepatitis of various genesis - primary sclerosing cholangitis - cystic fibrosis (cystic fibrosis) - nonalcoholic steatohepate - - biliary dyskinesia.
Contraindications
- size of cholesterol stones in the gallbladder more than 20 mm - presence of radiopaque (high calcium) gallbladder stones and common bile duct - gallbladder atrophy in gallstones, non-functioning gallbladder - biliary obstruction - acute inflammatory diseases of the gallbladder, bile ducts and intestines - cirrhosis in the stage of decompensation - severe liver failure - severe renal failure - pancreatitis (active phase) - pregnancy s - lactation - adults and children weighing up to 34 kg (for a given dosage form) - hypersensitivity to the drug.
Use during pregnancy and lactation
The drug is contraindicated during pregnancy and during breastfeeding.
Dosage and administration
The drug is prescribed inside. In case of difficulty swallowing, the capsule can be opened and its contents drunk down with a sufficient amount of liquid.When cholesterol gallstones dissolve, the capsules are taken in the evening, before bedtime, with a sufficient amount of liquid. The dose is approximately 10 mg / kg of body weight daily, which corresponds to: 2 capsules of the Ursoliv preparation in patients with a body weight of up to 60 kg; 3 capsules - in patients with body weight up to 80 kg; 4 capsules - in patients with body weight up to 100 kg; 5 capsules - in patients with a body weight over 100 kg. The duration of treatment is 6-12 months. To prevent re-formation of stones, it is recommended to take the drug for several months after the stones have dissolved. With symptomatic treatment of primary biliary cirrhosis, the daily dose depends on body weight and ranges from 2 to 6 capsules (from 10 to 15 mg of ursodeoxycholic acid per 1 kg of body weight). The drug is taken with food, washed down with a sufficient amount of liquid. The following regimen is recommended: Body weight Daily dose Morning Afternoon 34-50 kg 2 capsules 1 - 1 51-65 kg 3 capsules 1 1 1 66-85 kg 4 capsules 1 1 2 86-110 kg 5 capsules 1 2 2 More than 110 kg 6 capsules 2 2 2 For the treatment of biliary reflux gastritis, 1 capsule is prescribed 1 time / day before bedtime. The course of treatment - from 10-14 days to 6 months, if necessary - up to 2 years. In chronic hepatitis of various origins (toxic, medicinal and others), non-alcoholic fatty liver disease, incl. 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. In case of primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis), the average daily dose is 12-15 mg / kg; if necessary, the average daily dose may be increased to 20-30 mg / kg in 2-3 doses. The duration of therapy is from 6 months to several years. In biliary dyskinesia of the hypokinetic type, the average daily dose is 10 mg / kg in 2 doses for 2 weeks to 2 months. If necessary, the treatment is recommended to repeat.
Side effects
On the part of the digestive system: nausea, vomiting, pain in the epigastric region and right hypochondrium, constipation, transient increase in the activity of hepatic transaminases; rarely - diarrhea (may be dose-dependent), calcification of gallstones. In the treatment of primary biliary cirrhosis, transient decompensation of cirrhosis of the liver may occur, which disappears after discontinuation of the drug. Other: headache, malaise, myalgia, dizziness, allergic reactions (pruritus, urticaria, angioedema), exacerbation of previously existing psoriasis, alopecia.
Overdose
Cases of overdose UDCA still not described.
Interaction with other drugs
When used together, antacids containing aluminum and ion exchange resins (Kolestiramine) reduce the absorption of UDCA. With simultaneous use, lipid-lowering drugs (especially clofibrate), estrogens, neomycin, or progestogens (oral contraceptives) increase bile cholesterol saturation and may reduce the ability of ursodeoxycholic acid to dissolve cholesterol gallstones. With the simultaneous use of UDCA can increase the absorption of cyclosporine.
special instructions
To dissolve gallstones, UDCA calculus must be cholesterol (not radiopaque), no larger than 15–20 mm. At the same time, the gallbladder must remain functional, and the permeability of the cystic and common bile ducts must be maintained. When prescribing for the purpose of dissolving gallstones, it is necessary to monthly, and then every 3 months to conduct a biochemical blood test to determine the activity of hepatic transaminases, ALP, GGT, as well as the concentration of bilirubin. If you maintain high levels of the drug should be canceled. To control the effectiveness of treatment, it is recommended that every 6 months x-ray and ultrasound of the biliary tract be performed. When calcification of gallstones, a violation of the contractility of the gallbladder, or frequent bouts of biliary colic, treatment should be stopped. If within 6–12 months after the initiation of therapy, partial dissolution of the stones did not occur, it is unlikely that the treatment will be effective. Detection of a non-visualized gallbladder during treatment is evidence that the calculus did not completely dissolve, and treatment should be stopped. After complete dissolution of the stones, to exclude relapses, it is recommended to continue the use of UDCA for 3 months. Impact on the ability to drive motor vehicles and control mechanisms The drug does not adversely affect the ability to drive vehicles and / or other mechanisms.