Ursodeoxycholic acid

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[edit] BRAND NAMES

[edit] STRUCTURE

Ursodeoxycholic acid.jpg

[edit] MECHANISM OF ACTION

Ursodeoxycholic acid, a naturally occurring bile acid found in small quantities in normal human bile, decreases the cholesterol content of bile and bile stones by reducing the hepatic synthesis and secretion of cholesterol, and also by inhibiting the reabsorption of cholesterol by the intestines.

[edit] INDICATIONS

  • Radiolucent, noncalcified gallbladder stone dissolution
  • Prevention of gallstone formation in obese patients experiencing rapid weight loss (FDA approved)
  • Intrahepatic cholestasis of pregnancy
  • Primary biliary cirrhosis (PBC): PBC, is an autoimmune disease of the liver marked by the slow progressive destruction of the small bile ducts of the liver. When these ducts are damaged, bile builds up in the liver (cholestasis). Ursodeoxycholic acid helps reduce the cholestasis and improves blood test results (liver function tests)

[edit] DOSAGE

  • Gallbladder stone dissolution: 8-10 mg/kg/day given in 2 or 3 divided doses.
    Treatment requires months of therapy. Complete dissolution does not occur in all patients and recurrence of stones within 5 years has been observed in up to 50% of patients who do dissolve their stones on bile acid therapy.

[edit] CONTRAINDICATIONS

  • Presence of radiopaque, radiolucent bile pigment, or calcified cholesterol stones
  • Patients with compelling reasons for cholescystectomy including unremitting acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis or biliary-gastrointestinal fistula
  • Allergy to bile acids

[edit] PRECAUTIONS

  • Monitor AST, ALT at the initiation of therapy and thereafter as indicated by the particular clinical circumstances.
  • Obtain ultrasound images at 6 month intervals for the first year of therapy to monitor gallstone response. If gallstones appear to have dissolved, Ursodeoxycholic acid therapy should be continued and dissolution confirmed on a repeat ultrasound examination within 1-3 months. Most patients who eventually achieve complete stone dissolution will show partial or complete dissolution at the first on-treatment reevaluation. If partial stone dissolution is not seen by 12 months of Ursodeoxycholic acid therapy, the likelihood of success is greatly reduced.

[edit] INTERACTIONS

  • Decreased effect:
    • Bile acid sequestrants such as cholestyramine (Questran) and colestipol (Colestid) may interfere with the action of Ursodeoxycholic acid by reducing its absorption
    • Aluminum-containing antacids such as Maalox have been shown to adsorb bile acids, so they also may reduce Ursodeoxycholic acid absorption.
    • Estrogens, oral contraceptives, and clofibrate increase hepatic cholesterol secretion, and encourage cholesterol gallstone formation and hence may counteract the effectiveness of Ursodeoxycholic acid.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category B (US)
  • Nursing Mothers: It is not known whether Ursodeoxycholic acid is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when this drug is administered to a nursing mother.

[edit] SIDE EFFECTS

Possible adverse events are: Rash, pruritus, nausea, vomiting, diarrhea or pasty stools and headache

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[edit] REFERENCES