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Ursodiol: a cholesterol gallstone solubilizing agent.

C L Rosenbaum1, R J Cluxton

  • 1College of Pharmacy, University of Cincinnati, OH 45267.

Drug Intelligence & Clinical Pharmacy
|December 1, 1988
PubMed
Summary
This summary is machine-generated.

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Ursodiol effectively dissolves cholesterol gallstones by inhibiting hepatic cholesterol synthesis. This bile acid offers a favorable safety profile compared to chenodiol, with fewer adverse reactions like diarrhea.

Area of Science:

  • Hepatology
  • Gastroenterology
  • Pharmacology

Background:

  • Ursodiol is an FDA-approved bile acid for cholesterol gallstone dissolution.
  • It functions by reducing hepatic cholesterol synthesis and secretion.
  • Ursodiol metabolism results in less accumulation of potentially hepatotoxic lithocholic acid compared to chenodiol.

Purpose of the Study:

  • To evaluate the efficacy and safety of ursodiol in cholesterol gallstone dissolution.
  • To compare ursodiol's adverse reaction profile with that of chenodiol.

Main Methods:

  • The study focuses on the mechanism of action and clinical outcomes of ursodiol.
  • Data on patient response, gallstone dissolution rates, and adverse events are presented.
  • Comparison is made with chenodiol based on reported clinical data.

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Main Results:

  • Complete dissolution of cholesterol gallstones achieved in 17% of eligible patients.
  • Recurrence rates exceed 50% in initial responders.
  • Ursodiol exhibits a significantly lower incidence of diarrhea (4%) compared to chenodiol (up to 50%).
  • Elevated aspartate aminotransferase levels observed with chenodiol were not reported with ursodiol.

Conclusions:

  • Ursodiol is an effective treatment for select cholesterol gallstones.
  • Its improved safety profile, particularly reduced gastrointestinal side effects and lack of hepatotoxicity markers, presents a significant advantage over chenodiol.
  • These factors support ursodiol's consideration in hospital formularies for gallstone management.