Ursodeoxychole

Ursodeoxychole  

Ingredients
1 capsule contains:
Ursodeoxycholic acid – 250 mg

Pharmacological Group
Drugs used in gastrointestinal disorders.
Drugs that inhibit gallstone formation and facilitate their biliary excretion.

Pharmacological Action
Ursodeoxychole  is an ursodeoxycholic acid-containing drug.  Normally, ursodeoxycholic acid is contained in the bile in a small amount and is the least toxic and most hydrophilic acid bile among all other bile acids.
Administration of ursodeoxycholic acid reduces cholesterol synthesis in the liver and cholesterol absorption in the intestine. In addition, due to the formation of cholesteric liquid crystals ursodeoxycholic acid helps to dissolve cholesterol stones, to reduce bile lithogenicity and decrease cholate-cholesterol levels.
Ursodeoxychole, when administered in patients with cholestatic liver diseases, has a positive effect due to the replacement of  toxic bile acids with non-toxic  cytoprotective ursodeoxycholic acid, improvement of the hepatocyte secretion, and stimulation of immune regulatory processes.
In peroral administration ursodeoxycholic acid is quickly absorbed in the gastrointestinal tract, then bind to amino acids – glycine and taurine and excreted in the bile. Ursodeoxychole’s active ingredient  is cumulated in the bile; the cumulative level depends on the liver condition. Taking of ursodeoxycholic acid can result in some decrease of more lipophilic bile acid levels. Ursodeoxycholic acid is metabolized in the intestine and liver; excreted into the intestinal tract. The half-life of the active ingredient takes 3,5-5,8 days.

Indications
I. Diseases that manifest with cholestasis:  
Primary sclerosing cholangitis. Primary biliary cirrhosis.
Acute and chronic viral hepatitis.
Alcoholic liver disease.
Drug-induced  liver injuries (hormones, cytostatics, and etc.).
Congenital  ductopenia (intrahepatic bile duct hypoplasia, Alagille syndrome).
Mucoviscidosis (cystic fibrosis).
Hepatosis of pregnancy.
Neonatal cholestasis.
Parenteral nutrition induced cholestasis.
II. Diseases that do not manifest with cholestasis:
(with subclinical cholestasis).
Chronic hepatitis, including viral and alcoholic hepatitis.
Non-alcoholic steatohepatitis.
Cholelithiasis.
Biliary dyskinesia.
Biliary reflux gastritis and reflux esophagitis.
Prevention of cancer in patients with ulcerative colitis and Crohn's disease.

Use
Ursodeoxychole is for peroral administration. Do not crush or chew capsules before administration. Usually a single daily dose is used. It is recommended to take the drug with drinking water at night before going to bed. Administer Ursodeoxychole regularly for achieving therapeutic effect. The duration of treatment and dosage should be determined by the doctor.
In patients with cholesterol gallstones ursodeoxycholic acid dosage is 10 mg per kg of body weight per day.
Duration of treatment is 6-24 months. If no size of cholesterol gallstone size reduction occurred 12 months after the start of treatment with Ursodeoxychole the treatment should be discontinued.  
When administered in patients with bile reflux gastritis, the Ursodeoxychole dosage is 1 capsule a day.
Duration of treatment is 10-14 days. If necessary the doctor may extend the treatment period.
When administered in patients with primary biliary cirrhosis, the Ursodeoxychole dosage is 14 mg per kg of body weight per day. At the beginning of the treatment the daily dose of Ursodeoxychole should be divided into 3 administration (given that 1 capsule contains 250mg ursodeoxycholic acid), the most of it should be taken at night. When the liver condition is improved the daily dose of  Ursodeoxychole will be once a day before going to bed.
Duration of treatment with Ursodeoxychole in patients with primary biliary cirrhosis is unlimited. Sometimes at the beginning of treatment worsening of clinical symptoms might be observed; in such cases reduce the daily dose to 1 capsule and gradually increase to the desired therapeutic dose (dose increase should be done weekly by adding 1 capsule).

Side Effects
Administration of Ursodeoxychole in patients can cause the following side effects:
In the digestive tract and hepatobiliary system: pain in the liver (predominantly in patients with primary biliary cirrhosis), diarrhea, transient increase in liver enzymes, calcification of gallstones, vomiting.

Contraindications
Ursodeoxychole is contra-indicated in patients with known hypersensitivity reactions to ursodeoxycholic acid and additional ingredients contained in capsules.
Ursodeoxychole is contra-indicated in patients with acute inflammation of the gallbladder and biliary tract, biliary tract obstruction and gallbladder contractile function disorders.  
Ursodeoxychole is contra-indicated in patients having a gallbladder that is not visualized in radiological methods, as well as in patients with calcified stones and biliary colic.
Ursodeoxychole capsules are contra-indicated in patients with kidney and liver function disorders.
In pediatric practice Ursodeoxychole is used for treating children over 5 years old only.

Pregnancy
Ursodeoxychole is contra-indicated in the first trimester of pregnancy.  The drug should be administered in the second and third trimesters.  Before starting ursodeoxycholic acid treatment in women of childbearing age pregnancy should be excluded, and reliable contraception methods should be used during the entire treatment period.
If Ursodeoxychole should be administered during lactation, termination of breastfeeding should be considered.

Interaction with other drugs
Ursodeoxycholic acid absorption might decrease when administered in combination with colestipol, colestyramine and antacids containing aluminum hydroxide, aluminum oxide, and magnesium silicate.
If the drug should be administered in combination with these medications the interval between their intake should be at least 2 hours.
Combined administration of Ursodeoxychole improves intestinal cyclosporine adsorption (in concurrent administration the level of cyclosporine in plasma should be controlled with adjustment of its doses, if necessary).
Absorption of ciprofloxacin may be reduced when concurrently administered with ursodeoxycholic acid.
The effectiveness of ursodeoxycholic acid decreases when clofibrate, probucol, and bezafibrate are taken.  
In addition, ursodeoxycholic acid might become less effective when administering in patients taking peroral contraceptives and estrogens, as well as in patients on low-fat and high-cholesterol diet.