Hepatoprotective agent also has choleretic, cholelitolitic, lipid-lowering, cholesterol-lowering and immunomodulatory effects. It stabilizes hepatocyte membrane and cholangiocytes has a direct cytoprotective effect. As a result of the drug in the gastrointestinal circulation of bile acids content decreases hydrophobic (potentially toxic) acids. By reducing cholesterol absorption in the intestine and other biochemical effects having hypocholesterolemic action. Suppresses testosterone suspension reviews cell death caused by toxic bile acids.
With its high polar properties, ursodeoxycholic acid (UDCA) forms a non-toxic mixed micelles with apolar (toxic) bile acids, which reduces the ability of gastric reflyuktata damage cell membranes with biliary reflux gastritis and reflux esophagitis. In addition, UDCA forms double molecules that can be included in the composition of cell membranes, stabilize them and make immune to the effects of cytotoxic micelles. It reduces the saturation of bile cholesterol by inhibiting its absorption in the intestine, suppression of the synthesis in the liver and decrease secretion in the bile; increases the solubility of cholesterol in bile, forming with it the liquid crystals; It reduces the lithogenic index of bile. The result is the dissolution of cholesterol gallstones (a consequence of changes in the ratio of cholesterol / bile acids in bile) and preventing the formation of new stones (the result of reducing the content of cholesterol in bile). Induces cholepoiesis rich in bicarbonate, which leads to an increase in bile passages and stimulates the excretion of toxic bile acids through the intestine.
Immunomodulatory effect due to inhibition of the expression of HLA-antigens. (HLA – human leucocyte antigens – antigens histocompatibility) in the membranes of hepatocytes and cholangiocytes, normalization of natural killer activity of lymphocytes, etc. Significantly delay the progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis and alcoholic steatohepatitis, reduces the risk of development of esophageal varices.
Absorption and distribution.
UDCA in the jejunum absorbed by passive diffusion, and from the ileum by an active transport. It penetrates through the placental barrier. The concentration in plasma when administered 500 mg achieved after 30, 60, 90 min – 3.8, 5.5, 3.7 mmol / l, respectively. Distribution UDCA is characterized by a high degree of binding to plasma proteins, which may be 96-99%.
Metabolism and excretion.
As a result of the elimination of UDCA presistemna formed taurine and glycine conjugates, which are secreted into bile. Approximately 50-70% of the UDCA dose administered is excreted in the bile. The remainder of UDCA nevsosavsheysya fraction falls into the colon, where it undergoes bacterial cleavage (7-dehydroxylation) to give lithocholic acid. Lithocholic acid is partially absorbed from the gut, biotransformed in the liver and sulfolitoholilglitsinovy sulfolitoholiltaurinovy conjugates and excreted.
Indications for use:
- Primary biliary cirrhosis in the absence of signs of decompensation (symptomatic therapy);
- Dissolution of small and medium cholesterol stones in the gall bladder functioning;
- Biliary reflux gastritis and reflux esophagitis;
- Chronic hepatitis of various genesis;
- Alcoholic liver disease;
- Nonalcoholic steatohepatitis;
- Primary sclerosing cholangitis;
- Cystic fibrosis (cystic fibrosis);
- Biliary dyskinesia;
- Increased individual sensitivity to the drug;
- rentgenopolozhitelnye (high in calcium) gallstones;
- non-functioning gall bladder;
- acute inflammatory diseases of the gallbladder, bile ducts and intestines;
- cirrhosis of the liver in the stage of decompensation;
- expressed by the human kidney, liver, pancreas;
- lactose intolerance;
- lactase deficiency or glucose-galactose malabsorption;
- Children up to age 3 years.
With caution used in children aged 3 to 4 years, as possible difficulty in swallowing tablets, although ursodeoxycholic acid has no age restrictions apply.
Pregnancy and lactation:
The use of ursodeoxycholic acid during pregnancy is possible only when the expected benefit to the mother outweighs the potential risk to the fetus (adequate well-controlled studies of ursodeoxycholic acid in pregnant women has not been).
Data on the allocation of ursodeoxycholic acid in breast milk are not currently available. If necessary, the use of ursodeoxycholic acid during lactation should decide the issue of termination of breastfeeding.
Dosage and administration:
The tablets of the drug testosterone suspension reviews is taken orally without chewing, drinking plenty of water. The tablet can be divided in half.
For the dissolution of cholesterol gallstones average daily dose of the drug . The drug is taken in the evening before bedtime. The course of treatment – 6-12 months.To prevent the recurrence of stones is recommended taking the drug for a few months after the dissolution of stones.
Symptomatic treatment of primary biliary cirrhosis: an average daily dose – 10-15 mg / kg (if necessary – up to 20 mg / kg) from 6 months to several years. The drug is taken with food, drinking plenty of fluids.
When biliary reflux gastritis and reflux esophagitis , the dose is 10 mg / kg / day – 1 time a day at bedtime. The course of treatment – from 10-14 days to 6 months, if necessary – up to 2 years.
In chronic hepatitis of various genesis (toxic, drugs, etc..), The primary nealkogolnom steatohepatitis, alcoholic liver disease , the mean daily dose is 10-15 mg / kg body weight in 2-3 hours.The duration of therapy is 6-12 months or more.
The calcination gallstones, increased activity of “liver” enzymes, allergic reactions (including urticaria), diarrhea, nausea, abdominal pain; in the treatment of primary biliary cirrhosis may be a transient decompensation of cirrhosis of the liver, passing after discontinuation of the drug.
Cases of UDCA overdose are not known. Interaction with other drugs:
Interaction with other drugs
Do not use the drug at the same time with antacids containing aluminum and ion-exchange resins, as these drugs may interfere with the absorption of ursodeoxycholic acid.
With simultaneous use of lipid-lowering medications, estrogens, progestogens, or neomycin (oral contraceptives) increase the saturation of bile with cholesterol and may reduce the ability of ursodeoxycholic acid to dissolve cholesterol gallstones.
Ursodeoxycholic acid can enhance cyclosporine absorption from the intestine, which requires monitoring of cyclosporin blood concentration, and if necessary – its correct dosing regimen.
The successful dissolution requires that the stones were pure cholesterol, no larger than 15-20 mm, gallbladder filled with stones not more than half of the bile duct and retain their function.
When assigning to dissolve gallstones need to control the activity of “liver” transaminases and alkaline phosphatase, gamma-glutamyl, bilirubin concentrations. While maintaining high performance drug should be discontinued.
Holetsistografii should be performed every 4 weeks during the first 3 months of treatment in the future – every 3 months. Monitoring the effectiveness of the treatment carried out every 6 months during the ultrasound examination in the first year of therapy. After completely dissolving concrements encouraged to continue in use for at least three months, in order to facilitate the dissolution of calculi residues that are too small to be detected.
If within 6-12 months testosterone suspension reviews after initiation of therapy partial dissolution of stones did not happen, it is unlikely that treatment will be effective.
Detection during treatment nevizualiziruemaya gallbladder is a testament to the fact that the complete dissolution of the stones did not happen, and the treatment should be discontinued.
When calcified gallstones violation contractility of the gall bladder or frequent attacks of biliary colic treatment should be discontinued.
Effects on ability to drive and perform work that requires high concentration and speed of psychomotor reactions:
No data are available on the effect of UDCA on the ability to drive and use machines.