Cholelithiasis Medication
- Author: Douglas M Heuman, MD, FACP, FACG, AGAF; Chief Editor: Julian Katz, MD more...
Medication Summary
Medical dissolution of gallstones may be attempted with administration of ursodiol.
Gallstone Dissolution Agents
Class Summary
These agents suppress hepatic cholesterol synthesis and 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, 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 cholesterol synthesis and secretion and inhibits intestinal absorption. It appears to have little inhibitory effect on the synthesis and secretion into bile of endogenous bile acids and does not appear to affect 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.
Heuman DM, Moore EL, Vlahcevic ZR. Pathogenesis and dissolution of gallstones. In: Zakim D, Boyer TD, eds. Hepatology: A Textbook of Liver Disease. 1996. 3rd ed. Philadelphia, Pa: WB Saunders; 1996:376-417.
Center SA. Diseases of the gallbladder and biliary tree. Vet Clin North Am Small Anim Pract. May 2009;39(3):543-98. [Medline].
Portincasa P, Moschetta A, Palasciano G. Cholesterol gallstone disease. Lancet. Jul 15 2006;368(9531):230-9. [Medline].
[Best Evidence] Halldestam I, Kullman E, Borch K. Incidence of and potential risk factors for gallstone disease in a general population sample. Br J Surg. Nov 2009;96(11):1315-22. [Medline].
Shaffer EA. Epidemiology and risk factors for gallstone disease: has the paradigm changed in the 21st century?. Curr Gastroenterol Rep. May 2005;7(2):132-40. [Medline].
Wang HH, Liu M, Clegg DJ, Portincasa P, Wang DQ. New insights into the molecular mechanisms underlying effects of estrogen on cholesterol gallstone formation. Biochim Biophys Acta. Nov 2009;1791(11):1037-47. [Medline]. [Full Text].
Gilani SN, Bass G, Leader F, Walsh TN. Collins' sign: validation of a clinical sign in cholelithiasis. Ir J Med Sci. Aug 14 2009;[Medline].
Zaliekas J, Munson JL. Complications of gallstones: the Mirizzi syndrome, gallstone ileus, gallstone pancreatitis, complications of "lost" gallstones. Surg Clin North Am. Dec 2008;88(6):1345-68, x. [Medline].
Dauer M, Lammert F. Mandatory and optional function tests for biliary disorders. Best Pract Res Clin Gastroenterol. 2009;23(3):441-51. [Medline].
[Guideline] Katz DS, Rosen MP, Blake MA, et al; and Expert Panel on Gastrointestinal Imaging. ACR Appropriateness Criteria® right upper quadrant pain. [online publication]. Reston (VA): American College of Radiology (ACR). [Full Text].
Yao CC, Huang SM, Lin CC, Ho LC, Chang SW, Chen HM, et al. Assessment of common bile duct using laparoscopic ultrasound during laparoscopic cholecystectomy. Surg Laparosc Endosc Percutan Tech. Aug 2009;19(4):317-20. [Medline].
[Best Evidence] Mahid SS, Jafri NS, Brangers BC, Minor KS, Hornung CA, Galandiuk S. Meta-analysis of cholecystectomy in symptomatic patients with positive hepatobiliary iminodiacetic acid scan results without gallstones. Arch Surg. Feb 2009;144(2):180-7. [Medline].
[Guideline] NIH state-of-the-science statement on endoscopic retrograde cholangiopancreatography (ERCP) for diagnosis and therapy. NIH Consens State Sci Statements. Jan 14-16 2002;19(1):1-26. [Medline].
Binenbaum SJ, Teixeira JA, Forrester GJ, Harvey EJ, Afthinos J, Kim GJ, et al. Single-incision laparoscopic cholecystectomy using a flexible endoscope. Arch Surg. Aug 2009;144(8):734-8. [Medline].
Ghazal AH, Sorour MA, El-Riwini M, El-Bahrawy H. Single-step treatment of gall bladder and bile duct stones: a combined endoscopic-laparoscopic technique. Int J Surg. Aug 2009;7(4):338-46. [Medline].
[Guideline] Overby DW, Apelgren KN, Richardson W, Fanelli R. SAGES guidelines for the clinical application of laparoscopic biliary tract surgery. Surg Endosc. Oct 2010;24(10):2368-86. [Medline]. [Full Text].
Dan DV, Harnanan D, Maharaj R, Seetahal S, Singh Y, Naraynsingh V. Laparoscopic cholecystectomy: analysis of 619 consecutive cases in a Caribbean setting. J Natl Med Assoc. Apr 2009;101(4):355-60. [Medline].
Gurusamy K, Sahay SJ, Burroughs AK, Davidson BR. Systematic review and meta-analysis of intraoperative versus preoperative endoscopic sphincterotomy in patients with gallbladder and suspected common bile duct stones. Br J Surg. Jul 2011;98(7):908-16. [Medline].
Behar J, Corazziari E, Guelrud M, Hogan W, Sherman S, Toouli J. Functional gallbladder and sphincter of oddi disorders. Gastroenterology. Apr 2006;130(5):1498-509. [Medline].

