Udcacid 300

Ursodeoxycholic acid.

Each tablet contains ursodeoxycholic acid, BP 300 mg.

Pharmacology: Pharmacokinetics: Ursodeoxycholic acid is absorbed from the gastrointestinal tract and undergoes enterohepatic recycling. It is partly conjugated in the liver before being excreted into the bile. Under the influence of intestinal bacteria, the free and conjugated forms undergo 7α-dehydroxylation to lithocholic acid, some of which is excreted directly in the faeces and the rest is absorbed and mainly conjugated and sulfated by the liver before excretion. However, in comparison with chenodeoxycholic acid less ursodeoxycholic acid undergoes such bacterial degradation.
Pharmacodynamics: Bile acids are among the most important components of the bile and play a role in the stimulation of bile secretion. Bile acids are also important to keep the cholesterol in bile in solution. In a healthy person, the ratio between the concentration of cholesterol and bile acids in the bile is such that the cholesterol will remain in solution for most of the day. In this case, no gallstones can form (the bile is non-lithogenic). In patients with cholesterol stones in the bile, this ratio is changed and the bile is supersaturated with cholesterol (bile is lithogenic). This may cause a precipitation of cholesterol crystals and the formation of gallstones after some time.
The ursodeoxycholic acid converts lithogenic bile in non-lithogenic bile and gradually dissolves the cholesterol gallstones. Investigations of the effect of ursodeoxycholic acid on the cholestasis in patients with impaired biliary drainage and on the clinical symptoms in patients with primary biliary cholangitis and cystic fibrosis have shown that cholestatic symptoms in the blood (to be measured by the increased value of alkaline phosphatase (AF), gamma-GT and bilirubin) and the itch declined rapidly, while also the fatigue decreased in the majority of patients. Moreover, studies seem to indicate a positive benefit-risk ratio of the ursodeoxycholic acid in children and young adult cystic fibrosis patients with mild to moderate hepatobiliary disorders.
From clinical reports, long-term experience of 10 years and more has been gained with UDCA therapy in paediatric patients suffering from cystic fibrosis associated hepatobiliary disorders (CFAHD). There is evidence that treatment with changes, if it happens at an early stage of CFAHD. The treatment with UDCA should be started as soon as the CFAHD diagnosis is made in order to optimize the effectiveness of the treatment.

It is used for the dissolution of cholesterol-rich gallstones in patients with functioning gall bladders. It is also used in primary biliary cirrhosis.

Adult: 300 mg, three times a day with meals.
Or as prescribed by the physician.

In the case of overdose, diarrhea may occur. In general, other symptoms of overdose are unlikely, because the absorption of the ursodeoxycholic acid decreases with increasing dose and therefore more is excreted in the faeces.
If diarrhoea occurs, the dosage should be reduced and treatment should be discontinued in case of persistent diarrhoea.
No specific measures are needed and the consequences of diarrhoea should be treated symptomatically with restoration of fluid and electrolyte balance.

Do not administer the drug to the following patients: Patients with hypersensitivity to its components; patients with complete obstruction of biliary tract (choleretic actions may aggravate the symptoms); patients with fulminant hepatitis; patients with radiopaque calcifying cholelithiasis; patients with nonfunctioning gall bladder or acute cholecystitis; pregnant women or women suspected of being pregnant; pediatric patients; patients with renal disease; patients with gastric ulcers (acute gastroduodenal ulcers); patients with colitis or enteritis such as Crohn's disease.

Careful administration should be exercised in case that the patients with jaundice and hepatic cirrhosis. Regularly check the level of liver enzymes (ALT, AST, γ-GT, ALP, total bilirubin). There is a faint chance that an overdose causes a severe adverse event. If necessary, perform liver function test. There is no evidence that dose adjustment in geriatric patients is necessary. However, appropriate precautions should be exercised such as reducing the dose because the physical functions in elderly patients generally declines.

Ursodeoxycholic acid should not be given to patients with peptic ulcer disease, inflammatory bowel disease, or chronic liver disease. Its use should be avoided in pregnancy.
General Precautions: The following patients should see a physician before taking this drug: Patients with severe pancreatic disease; patients with choledocholithiasis; patients with variceal bleeding, hepatic encephalopathy, ascites and those in need of an urgent liver transplantation.

Pregnancy: There are no or limited amount of data from the use of ursodeoxycholic acid in pregnant women. Studies in animals have shown reproductive toxicity during the early gestation phase. Ursodeoxycholic acid must not be used during pregnancy, unless clearly necessary.
Women of childbearing potential: Women of childbearing potential should be treated with ursodeoxycholic acid, only if they practice reliable contraception, non-hormonal contraceptives or oral contraceptives with low oestrogen dose are recommended. However, in patients taking ursodeoxycholic acid for dissolving gallstones, an effective non-hormonal contraception should be used, since hormonal oral contraceptives may increase biliary lithiasis. The possibility of a pregnancy must be excluded before beginning treatment.
Breastfeeding: According to few documented cases of breastfeeding women, milk levels of ursodeoxycholic acid levels in milk are very low and probably no adverse reactions are to be expected in breastfed infants.
Fertility: Animal studies did not shown an influence of ursodeoxycholic acid on fertility. Human data on fertility treatment with ursodeoxycholic acid are not available.

Diarrhea, vomiting, nausea, abdominal pain, constipation, heartburn, epigastric discomfort.
Hypersensitivity: Itchiness, rashes.
Interstitial Pneumonia: Fever, cough, dyspnea.
Rarely, general malaise, dizziness, calcification of cholelithiasis, increase in ALT, ALP, AST, γ-GT, decrease in leukocyte.
Increase in serum bilirubin.

Concurrent administration of oral hypoglycemic agent (Tolbutamide); should be cautiously administered to patients with diabetes because ursodeoxycholic acid may increase the effects of oral hypoglycemic agents. 
The following may reduce the absorption of this drug: Cholestyramine, cholestipol, charcoal, aluminum hydroxide and magnesium-based antacids; cholesterol-reducing drugs in bile (e.g. Oral contraceptives containing estrogens) or cholesterol-reducing drugs in serum (e.g. clofibrate); drugs which induce liver injury.

Store at temperatures not exceeding 30°C.

Cholagogues, Cholelitholytics & Hepatic Protectors

A05AA02 - ursodeoxycholic acid ; Belongs to the class of bile acids. Used in bile therapy.

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