Gallstones (Cholelithiasis) Medication

Updated: Apr 01, 2019
  • Author: Douglas M Heuman, MD, FACP, FACG, AGAF; Chief Editor: BS Anand, MD  more...
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Gallstone Dissolution Agents

Class Summary

These agents suppress hepatic cholesterol secretion and inhibit intestinal absorption of cholesterol. Ursodiol is the most common drug used. It solubilizes cholesterol in micelles and acts by dispersing cholesterol in aqueous media.

Ursodiol (Actigall, Urso 250, Urso Forte)

Ursodiol (ursodeoxycholic acid) is indicated for radiolucent noncalcified gallbladder stones smaller than 20 mm in diameter when conditions preclude cholecystectomy. Ursodiol suppresses hepatic secretion and inhibits intestinal absorption of cholesterol. It appears to have little inhibitory effect on the synthesis and secretion into bile of endogenous bile acids and does not appear to affect the secretion of phospholipids into bile. After repeated doses, the drug reaches steady-state bile concentrations in about 3 weeks. Cholesterol is insoluble in aqueous media, but it can be solubilized in at least 2 different ways in the presence of dihydroxy bile acids. In addition to solubilizing cholesterol in micelles, ursodiol acts by dispersing cholesterol as liquid crystals in aqueous media. The overall effect of ursodiol is to increase the concentration level at which saturation of cholesterol occurs.

The various actions of ursodiol combine to change the bile of patients with gallstones from cholesterol-precipitating to cholesterol-solubilizing bile, thus resulting in bile conducive to cholesterol stones dissolution.