Ursodeoxycholic Acid

Indications
 Oral
Dissolution of cholesterol-rich gallstones
Adult: 6-12 mg/kg daily as a single dose at bedtime or in 2-3 divided doses continued for 3-4 mth after radiological disappearance of stones. Doses may be divided unequally with a higher dose given before bedtime to counteract increase in biliary cholesterol saturation which occurs in early morning. Max: 15 mg/kg.
Hepatic impairment: Chronic liver disease (except primary biliary cirrhosis): use with caution.
Oral
Primary biliary cirrhosis
Adult: 10-15 mg/kg daily in 2-4 divided doses.
Oral
Prophylaxis of gallstones in patients undergoing rapid weight loss
Adult: 300 mg bid.
Hepatic impairment: Chronic liver disease (except primary biliary cirrhosis): use with caution.
Contraindications
 Calcified and pigment gallstones, radio opaque gallstones. Nonfunctioning gall bladders; chronic liver and peptic ulcer disease. Inflammatory disease of colon and small intestine. Pregnancy.
Warnings / Precautions
 50% of successfully treated patients will develop further gallstones within 10 yr. Lactation.
Adverse Reactions
 Diarrhoea, pruritus, nausea, vomiting, gallstone calcification.
Drug Interactions
 Cholestyramine, charcoal and antacids may reduce effectiveness. Aluminum-based antacids may reduce absorption. Oestrogens and clofibrate may counteract effectiveness of ursodeoxycholic acid by increasing cholesterol elimination in bile. Possible increase in ciclosporin serum concentration. Decreased effectiveness of dapsone. Possible decrease in serum ciprofloxacin and nitrendipine.
See Below for More ursodeoxycholic acid Drug Interactions
Mechanism of Actions
 Ursodeoxycholic acid suppresses hepatic synthesis and secretion of cholesterol and also inhibits intestinal absorption of cholesterol.
Absorption: Rapidly and completely absorbed from the GI tract.
Distribution: Protein binding: 96-98%. Undergoes enterohepatic recycling.
Metabolism: Partly conjugated in the liver before being excreted into the bile. Free and conjugated forms undergo 7a-dehydroxylation to lithocholic acid under the influence of gut bactera. Some are reabsorbed and then further conjugated and sulfated by the liver.
Excretion: Faeces.
Administration
 Should be taken with food.
ATC Classification
 A05AA02 - ursodeoxycholic acid ; Belongs to the class of bile acids.
Available As
  • Ursodeoxycholic Acid 150 mg
  • Ursodeoxycholic Acid 250 mg
  • Ursodeoxycholic Acid 300 mg
  • Ursodeoxycholic Acid 450 mg
  • Ursodeoxycholic Acid 500 mg
  • Ursodeoxycholic Acid 600 mg
  • Ursodeoxycholic Acid 75 mg

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