Ursodeoxycholic Acid

Indications

Ursodeoxycholic Acid is used for: Dissolution of cholesterol-rich gallstones, Primary biliary cirrhosis, Prevention of gallstone formation in obese patients experiencing rapid weight loss,

Adult Dose

Oral Dissolution of cholesterol-rich gallstones Adult: 8-12 mg/kg once daily at bedtime or in 2 divided doses continued for 3-4 mth after radiological disappearance of gallstones. Duration of treatment: Up to 2 yr. Obese patients: Up to 15 mg/kg daily. Primary biliary cirrhosis Adult: 10-16 mg/kg daily in 2-4 divided doses, may be taken once daily in the evening after the 1st 3 mth. Prophylaxis of gallstones in patients undergoing rapid weight loss Adult: 300 mg bid. Non-alcoholic fatty liver disease: 13-15 mg/kg/day;

Child Dose

Renal Dose

Administration

Should be taken with food.

Contra Indications

Acute inflammation of gallbladder or biliary tract, occlusion of biliary tract, frequent episodes of biliary colic, radio-opaque calcified gallstones, impaired contractility of gallbladder, non-functioning gallbladder, inflammatory bowel disease, hepatic and intestinal conditions interfering w/ enterohepatic recirculation of bile acids, extrahepatic and intrahepatic cholestasis, ileal resection and stoma, regional ileitis, active duodenal and gastric ulcer; acute, chronic or severe hepatic disease.

Precautions

Excessive diatery intake of calories and cholesterol should be avoided. Liver function tests and bilirubin levels should be monitored every month for three months after start of therapy. 50% of successfully treated patients will develop further gallstones within 10 yr. Pregnancy and lactation. Monitoring Parameters Monitor LFTs mthly for the 1st 3 mth and every 6 mth thereafter. Lactation: unknown if excreted in breast milk; use caution

Pregnancy-Lactation

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.

Adverse Effects

Side effects of Ursodeoxycholic Acid : >10% Headache, Dizziness, Diarrhea, Dyspepsia, Nausea/vomiting, Back pain, Upper respiratory tract infection 1-10% Alopecia, Rash, Hyperglycemia, Flatulence, Peptic ulcer, Urinary tract infection, Leukopenia, Thrombocytopenia, Cholecystitis >1% Fatigue, Abdominal pain, Thrombocytopenia, Pruritus, Angioedema, Peripheral edema, Biliary pain

Mechanism of Action

Ursodeoxycholic acid suppresses hepatic synthesis and secretion of cholesterol and also inhibits intestinal absorption of cholesterol.