Gallstone Solubilizers

Class Summary

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

Ursodiol (Actigall, URSO, Ursofalk)

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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.

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Media Gallery

Pediatric Gallstones (Cholelithiasis). Transverse view of the gallbladder reveals multiple stones, without gallbladder wall thickening, edema, or surrounding fluid accumulation.

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Author

Melissa Kennedy, MD Attending Physician, Division of Gastroenterology, Hepatology, and Nutrition, Children's Hospital of Philadelphia

Melissa Kennedy, MD is a member of the following medical societies: American Academy of Pediatrics, North American Society for Pediatric Gastroenterology, Hepatology and Nutrition

Disclosure: Nothing to disclose.

Coauthor(s)

Joshua R Friedman, MD, PhD Director and Head of Disease Biology, Janssen Research and Development

Joshua R Friedman, MD, PhD is a member of the following medical societies: American Academy of Pediatrics, American Association for the Study of Liver Diseases, North American Society for Pediatric Gastroenterology, Hepatology and Nutrition

Disclosure: Received salary from Johnson & Johnson for employment.

Specialty Editor Board

Mary L Windle, PharmD Adjunct Associate Professor, University of Nebraska Medical Center College of Pharmacy; Editor-in-Chief, Medscape Drug Reference

Disclosure: Nothing to disclose.

B UK Li, MD Professor of Pediatrics, Division of Gastroenterology, Hepatology and Nutrition, Medical College of Wisconsin; Attending Gastroenterologist, Director, Cyclic Vomiting Program, Children’s Hospital of Wisconsin

B UK Li, MD is a member of the following medical societies: Alpha Omega Alpha, American Gastroenterological Association, North American Society for Pediatric Gastroenterology, Hepatology and Nutrition

Disclosure: Nothing to disclose.

Chief Editor

Carmen Cuffari, MD Associate Professor, Department of Pediatrics, Division of Gastroenterology/Nutrition, Johns Hopkins University School of Medicine

Carmen Cuffari, MD is a member of the following medical societies: American College of Gastroenterology, American Gastroenterological Association, North American Society for Pediatric Gastroenterology, Hepatology and Nutrition, Royal College of Physicians and Surgeons of Canada

Disclosure: Received honoraria from Prometheus Laboratories for speaking and teaching; Received honoraria from Abbott Nutritionals for speaking and teaching. for: Abbott Nutritional, Abbvie, speakers' bureau.

Acknowledgements

The authors and editors of Medscape Reference gratefully acknowledge the contributions of previous authors Alexandre F Migala, DO, Hildegardo Costa, MD, and Richard D Warren, MD, to the development and writing of the source article.