URSODEOKSIHOLEVAYA ACID (Ursodeoxycholic acid)

     Chemical name: (3 alpha 5 beta, beta 7) -3,7-edge Digidroksiholan-24- acid

     Description: Primary gall acid, normally in the human body produtsiruetsya in small quantities and is about 5% of the total pool of biliary acids in significant concentrations determined in extracts of some bears. The white or slightly yellow powder, which consists of crystalline particles bitter taste. Free soluble in ethanol, glacial acetic acid, little soluble in chloroform, it is difficult to dissolve in the air, almost nerastvorim water.

     Pharmacology: Farmakologicheskoe action-holelitoliticheskoe, zhelchegonnoe, gepatoprotektivnoe, gipoholesterinemicheskoe, immunomoduliruyuschee.

Stabilizes hepatocyte membrane and holangiotsitov, tsitoprotektivnoe has a direct effect. As a result of LS on gastrointestinal infection circulation biliary acid content decreases chemicals (potentially toxic) acids. By reducing cholesterol intake in the intestine and other biochemical effects have gipoholesterinemicheskoe effect. Inhibit cell death caused by toxic biliary acid.

With high polar properties ursodeoksiholevaya acid (UDHK) is a non-toxic mixed with Micelle apolyarnymi (toxic) biliary acid, which reduces the ability of digestive reflyuktata damage cell membranes in the biliary gastritis and reflux esophagitis ezofagite. In addition, UDHK is a double molecule that can be included in the composition of cell membranes, stabilize it and make impervious to the actions tsitotoksichnyh Mitzell. Reduces cholesterol saturation extracts from oppression its removal bowel, suppress synthesis in the liver and reduced secretion of bile; Solubility increases cholesterol in the bile, forming its liquid crystals; Reduces litogenny index insight. The result is dissolving holesterinovyh biliary stones (a change in the ratio of cholesterol / biliary bile acid), and prevention of new konkrementov (a reduction of cholesterol in the bile). Induces holerez rich bikarbonatami, resulting in an increase in export and encourage passage down biliary toxic acids through the bowel.

Immunomoduliruyuschee due to the oppression HLA- antigen expression in hepatocyte membrane and holangiotsitov, normalization of natural killernoy activity lymphocytes and other Dostoverno delaying the progression of fibrosis in patients of primary biliary cirrhosis, and purchased alcohol steatogepatitom, reduces the risk of developing varicose vein problems oesophagus.

When you receive inside absorbed in the intestine disease by passive diffusion, and the face height through active transport. Cmax achieved after 1-3 h. Linking with high protein (from healthy volunteers with protein linked to at least 70% nekonyugirovannoy UDHK). With systematic admission UDHK gall is the main acid in serum and about 48% of the total biliary acid in the blood. Included in the gastrointestinal infection circulation. In liver UDHK associated with glycine and meals; Formed konyugaty sekretiruyutsya in animals. Therapeutic effect depends on the concentration of bile UDHK; Against the backdrop of therapy is dozozavisimoe increase its share in the pool biliary acids to 50-75% (with daily doses of 10-20 mg / kg). Passes through the placenta barrier. Report the predominantly with faeces, very small number (less than 1%) with urine. A small number nevsosavsheysya UDHK thick in diameter has been split bacteria (7-degidroksilirovanie) to litoholevoy acid, which is partly absorbed from the colon, liver and sulfatiruetsya to quickly return to the faeces of sulfotilholilglitsinovogo or sulfotilholiltaurinovogo konyugatov.

     Application: Holesterinovye stones in the gall bladder, hepatitis (chronic, including atypical forms Poniard chronic, acute viral), nealkogolny steatogepatit, toxic (including alcohol, drugs) damage the liver, primary biliary cirrhosis and liver fibrosis, primary sclerosing holangit, biliary atresia vnutripechenochnyh ways holestaz with parenteral nutrition, biliary dyskinesia ways, biliary reflux gastritis and reflux esophagitis; chronic opistorhoz; prevention of liver damage using hormonal contraceptives and drugs.

     Contraindications: Hypersensitivity, acute inflammatory diseases of the gall bladder, bowel and biliary ducts, complete biliary tract obstruction, obyzvestvlennye biliary stones, cirrhosis of the liver decompensation stage expressed violations as kidney, pancreas.

     Restrictions apply to: Children's age (research holelitoliticheskogo UDHL effect of age children are not held). Studies in children with the disease holestaticheskimi atreziey liver and biliary ducts have not identified specific paediatric problems, which restrict the use of medicines in children.

     Application of pregnancy and breast feeding: When pregnancy is possible if the expected effect of therapy over the potential risk to the fetus (adequate and well-controlled study of safety in pregnant women did not). A nursing care in the appointment of women (not known whether enters LS in breast milk).

     Adverse actions: Constipation or Diarrhoea, nausea, pain in the area and the right epigastralnoy podrebere, calcination biliary stones, improving the liver transaminaz, allergic reactions (plasma and skin itching). When treating primary biliary cirrhosis may experience some temporary decompensation hepatic cirrhosis, which disappears after the LS.

     Networking: Alyuminiysoderzhaschie antatsidy, kolestiramin and kolestipol linked ursodeoksiholevuyu acid in the bowel, reducing its intake and decrease efficiency. Gipolipidemicheskie LS (especially klofibrat), estrogen, neomycin, progestin may increase the saturation of bile cholesterol and reduce the ability UDHK dilute holesterinovye biliary konkrementy.

     Dosing and Administration: inside (not razzhevyvaya and vine enough liquid). Treatment dosing and duration of treatment are set individually; The average dose of 8-10 mg / kg / day.

     Precautions: The long (more than 1 month) treatment requires monthly monitoring of liver transaminaz, SCHF, gamma glutamiltransferazy and bilirubin in the blood (especially in the first 3 months therapy). The effectiveness of the treatment according to their radiological studies and ultrasound apparatus ways (every six months). To prevent a recurrence of cholelithiasis should continue treatment several months after dissolution of stones.

During treatment of women of childbearing age should be reliable methods of contraception.

     Special instructions: Positive results can be obtained only if there is a holesterinovyh (rentgenonegativnyh) biliary stones smaller than 15-20 mm, and saved as gall bladder and road cystic duct and gall general.

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