Ursodeoxycholic acid: instructions for use, analogues, reviews

Recently, ursodeoxycholic acid has been increasingly used to treat various liver lesions. The instruction for the use of this chemical compound indicates its effectiveness in many serious diseases. What is this substance? What is ursodeoxycholic acid intended for? In which products is it present?

Description

Ursodeoxycholic acid, the use of which is based on its origin and properties, is a white-yellow crystalline powder. It has a bitter taste. This substance in a normally functioning human body is produced in small amounts. Its specific gravity is approximately 5% of the total mass of bile acids. It is hydrophilic and does not have cytotoxicity. This chemical compound is soluble in alcohol and acetic glacial acid, slightly soluble in chloroform and practically insoluble in water. Ursodeoxycholic acid in products is not contained. It is found in the gallbladder of a brown bear.

Ursodeoxycholic acid (UDCA) is an epimer of chenodeoxycholic acid. Initially, it was used to treat reflux gastritis and cleavage of gallstones. Over time, it began to be used in many other diseases. UDCA is considered the safest bile acid.

The action of ursodeoxycholic acid

To date, the use of UDCS is the standard for the treatment of various cholestatic liver diseases with an autoimmune component. The mechanism of action of this agent is to stabilize the cells of this organ. Its molecules can be embedded in the membranes of liver cells - hepatocytes. Due to this they are able to make them more resistant to the action of aggressive factors. This hepatoprotective agent has a choleretic effect. UDCS reduces the synthesis of cholesterol in the liver and prevents its absorption in the intestine. This drug reduces the lithogenicity of bile and increases the acid content in it. It improves lipase activity, pancreatic and gastric secretion. Ursodeoxycholic acid has a hypoglycemic effect, stimulates the formation and separation of bile, reduces the level of cholesterol in it.

This drug is conducive to partial or complete cleavage of cholesterol stones. That is why it is used more often. Connecting with cholesterol, it increases the solubility of its crystals, which acts destructively on gallstones. UDCA has an immunomodulatory effect, which consists in increasing lymphocyte activity, reduces the expression of various antigens on membranes of hepatocytes. It affects the number of T-lymphocytes, reduces the number of eosinophils.

UDCA reduces the concentration of cholesterol in bile by its dispersion and the transition of this substance to the liquid-crystalline phase. It affects the enterohepatic circulation of bile salts. As a result, reabsorption in the intestine of endogenous hydrophobic and toxic compounds decreases. This drug has a direct hepatoprotective and choleretic effect. Ursodeoxycholic acid, reviewed by specialists in the field of hepatology testify to its effectiveness, is able to reduce liver fibrosis with its fatty degeneration.

Application

Ursodeoxycholic acid, the use of which is carried out under the supervision of the attending physician, is prescribed in such pathological conditions:

• the presence of cholesterol stones localized in the gallbladder or common duct;

• impossibility of treatment by endoscopic or surgical method;

• chronic, atypical, acute and autoimmune hepatitis ;

• the presence of cholesterol stones after mechanical and extracorporeal lithotripsy;

• Toxic (medicinal, alcoholic) liver damage;

• sclerosing cholangitis;

• primary biliary cirrhosis without signs of decompensation;

Atresia of the biliary tract;

• cystic fibrosis;

• chronic active hepatitis;

• cholestasis with parenteral nutrition;

• biliary dyskinesia;

• biliary dyspeptic syndrome with biliary dyskinesia and cholecystopathy;

• chronic opisthorchiasis;

Congenital atresia of bile ducts;

• Biliary reflux-esophagitis and reflux gastritis.

Ursodeoxycholic acid (UDCA) is also used to prevent liver damage caused by taking cytotoxic drugs and hormonal contraceptives. It is prescribed for other diseases caused by congestion of bile. UDCS is prescribed for auxiliary treatment for liver or other organs transplantation.

Contraindications

Ursodeoxycholic acid, whose reviews are mostly positive, has serious contraindications. These include:

• inflammatory diseases of the gallbladder, intestines and bile ducts in the acute phase;

• X-ray positive gallstones with a high calcium content;

• biliary tract obstruction;

• hypersensitivity;

• cirrhosis of the liver during decompensation;

• Crohn's disease;

• pronounced disorders in the functioning of the pancreas, liver and kidneys.

Restrictions on use

Ursodeoxycholic acid, the instruction for its use clearly indicates the absence of strict limitations in its use, is not prescribed for children under 3 years in capsule form. For their treatment, suspensions containing this drug substance are used. So far, specialists have not carried out relevant studies aimed at determining the chololitholytic effect of this substance depending on the age of the child. At the same time, studies on children with atresia of the bile duct and some liver diseases showed no specific pediatric problems.

Drugs containing ursodeoxycholic acid are prescribed to pregnant women only when the estimated effect of therapy with this drug exceeds the potential risk for the unborn child. At the same time, we should not forget that no one has conducted full-fledged scientific research on the safety of this substance for this category of patients. Since it is not known whether UDCA penetrates into breast milk, care should be taken in prescribing this drug to lactating women.

Side effects

Ursodeoxycholic acid, the instruction for its use indicates not only limitations in its use, but also on possible side effects, can lead to such pathological phenomena as:

• constipation, diarrhea;

• nausea;

• increased activity of transaminases;

• pain in the right hypochondrium and epigastric region;

• allergic reactions to the skin (itching, rash);

• Calcination of stones.

Treatment of primary biliary cirrhosis with this drug sometimes leads to the fact that the patient has a transient decompensation that disappears after the withdrawal of this drug.

Precautionary measures

For the successful litholysis of cholesterol stones with the help of UDCA, the following conditions must be taken into account:

• their size does not exceed 2 cm;

• they do not give a shadow on the radiograph;

• the gallbladder functions normally;

• ducts retain patency;

• the bubble is filled with stones less than half;

• common bile duct contains no stones.

What other restrictions does ursodeoxycholic acid have? The instruction to this medical product indicates that with prolonged treatment, which is more than 1 month, it is necessary to conduct regular (once in 30 days) monitoring of hepatic transaminases, phosphatase, bilirubin, gamma-glutamyltransferase. Conducting such analyzes is especially important in the initial 3 months of therapy with UDCS. The effectiveness of treatment is confirmed every six months by x-ray and ultrasound examination of biliary excrements. To prevent attacks of recurrence of cholelithiasis, treatment is continued after complete dissolution of the stones. It can last many months.

During treatment of UDCS, women of childbearing age are recommended to use reliable methods of protection from pregnancy. These can be non-hormonal drugs or contraceptives with a small amount of estrogens.

Form release and dosage

Ursodeoxycholic acid, the instruction for its use gives a detailed description of the regimens for its administration, is available in such dosage forms:

• capsules and tablets of 150 and 250 mg;

• suspension for children.

Dosage of ursodeoxycholic acid is established strictly individually. It depends on the severity of a person's condition and body weight. Most often it is prescribed at 10-20 mg / kg per day. This dose is taken at a time, in the evening. The duration of therapy directly depends on the indications. This drug is absorbed in the small intestine, and after 3 hours in the blood plasma, its highest concentration is noted. The constant intake of medicaments containing ursodeoxycholic acid makes it the main bile acid in the human body. This substance undergoes a number of transformations and in the final result is excreted as metabolites with feces and urine.

The duration of therapy is determined by the attending physician. It can be different depending on the type of disease. In some particularly severe cases, the use of UDCA drugs lasts for years.

Interaction with other drugs

With the joint administration of UDCA and "Cyclosporine," the absorption of the latter is unpredictably increased. At the same time, blood plasma concentration sharply increases the concentration of these drugs. In rare cases of taking UDCS simultaneously with the drug "Ciprofloxacin" the concentration of the latter decreases.

Ursodeoxycholic acid (analogs)

Ursodeoxycholic acid (capsules, tablets) is available under different names. Such means differ among themselves with the auxiliary substances that make up their composition. So, on sale it is possible to meet the following medicines with ursodeoxycholic acid:

• Capsules "Ursosan", intended for the treatment of diffuse liver diseases, cholelithiasis, with biliary reflux gastritis and reflux esophagitis, primary cirrhosis, medicinal and toxic liver damage, cholecystectomy, alcoholic disease, sclerosing cholangitis, bile duct atresia, non-alcoholic steatohepatitis. Ursodeoxycholic acid ("Ursosan") is also used to prevent liver damage.

• Tablets "Ukrliv", which are taken with hepatic insufficiency, chronic hepatitis, cholelithiasis.

• Capsules "Ursofalk", appointed for various diseases of the gallbladder and liver, accompanied by cholestasis, a decrease in certain liver functions, increased cholesterol levels. These include: primary biliary cirrhosis and sclerosing cholangitis, reflux gastritis and reflux esophagitis, hepatitis of various etiologies, cholesterol stones, cystic fibrosis, various liver lesions, bile stasis. This drug is used as a preventative against liver damage when taking strong drugs.

• Ursodex tablets, which are taken with biliary cirrhosis without signs of decompensation and reflux gastritis. They are used to dissolve small cholesterol stones in the normal functioning of the gallbladder.

• Capsules "Ursodez", used for cleavage of cholesterol stones, treatment of reflux gastritis, for symptomatic therapy with primary cirrhosis of the liver without signs of decompensation.

• Capsules "Ursolizin", designed to dissolve cholesterol stones and symptomatic therapy of biliary cirrhosis, gallbladder cholesterosis and reflux gastritis. The drug is used in complex therapy for the treatment of patients with chronic hepatitis and cirrhosis of the liver.

• Capsules "Holudexan", used to treat uncomplicated cholelithiasis, chronic active hepatitis, alcohol and toxic liver damage, non-alcoholic steatohepatitis, primary biliary cirrhosis, primary sclerosing cholangitis, cystic fibrosis, bile duct dyskinesia, reflux gastritis and reflux esophagitis.

• Capsules "Urdoksa", which are prescribed for primary biliary cirrhosis without signs of decompensation, reflux gastritis. The drug well dissolves small and medium cholesterol stones while maintaining the normal function of the gallbladder.

• Capsules "Ursoror S", prescribed for uncomplicated cholelithiasis, primary cirrhosis, acute and chronic hepatitis, sclerosing cholangitis, intrahepatic atresia, reflux gastritis and reflux esophagitis, cholestasis, parenteral nutrition, biliary dyskinesia, liver pathology, Cystic fibrosis, fatty hepatosis, dyspeptic syndrome. The drug is used to prevent liver damage when using hormonal contraceptives and cytostatics, the formation of stones in obesity.

Ursodeoxycholic acid, analogues of this substance are taken only for the purpose of the attending physician.