Pediatric Gallstones (Cholelithiasis) Medication

Updated: Mar 30, 2021
  • Author: Melissa Kennedy, MD; Chief Editor: Carmen Cuffari, MD  more...
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Gallstone Solubilizers

Class Summary

These agents are indicated for the treatment of radiolucent, noncalcified gallbladder stones.

Ursodiol (Actigall, URSO, Ursofalk)

Also called ursodeoxycholic acid, this drug is indicated for radiolucent, noncalcified gallbladder stones less than 20 mm in diameter, when conditions preclude cholecystectomy. Ursodiol suppresses hepatic cholesterol synthesis and secretion and also inhibits intestinal absorption. It appears to have little inhibitory effect on synthesis and secretion into bile of endogenous bile acids and does not appear to affect secretion of phospholipids into bile. After repeated doses, ursodiol reaches steady-state bile concentrations in about 3 weeks.

Cholesterol is insoluble in aqueous media but 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 the 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 the dissolution of cholesterol stones.

Ursodiol is used in combination with chenodeoxycholic acid and in conjunction with extracorporeal shock-wave lithotripsy for the dissolution of gallstones. It is also indicated for gallstone prevention. Ursodiol is not FDA-approved for children, but data are emerging.

Ursodiol is available in 250-mg and 500-mg tabs and in 300-mg caps. It is also available as an orphan drug (Ursofalk) in 60 mg/mL suspension. An extemporaneous liquid formulation may be compounded for pediatric use.