Biliary Disease Medication

Updated: May 02, 2018
  • Author: Annie T Chemmanur, MD; Chief Editor: BS Anand, MD  more...
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Medication Summary

The goals of pharmacotherapy are to reduce morbidity and to prevent complications.


Gallstone dissolution agents

Class Summary

Ursodeoxycholic acid is a naturally occurring bile acid used successfully in the dissolution of gallstones, microlithiasis, and in primary biliary cirrhosis. Some benefit may exist in patients with Caroli disease.

Ursodiol (Actigall)

Decreases cholesterol content of bile and bile stones probably by reducing the secretion of cholesterol from the liver and the amount reabsorbed by intestines. It is also used for PBC since it displaces endogenous bile acids from the enterohepatic circulation, stabilizes hepatocellular membranes, and reduces the abnormal expression of HLA class I and II molecules on the hepatocytes.


Farnesoid X Receptor Agonist

Class Summary

The farnesoid X receptor (FXR) is a nuclear receptor expressed in the liver, intestine, kidney, and adipose tissues that regulates a wide variety of target genes critically involved in the control of bile acid synthesis and transport, lipid metabolism, and glucose homeostasis.

Obeticholic acid (Ocaliva)

Farnesoid X receptor (FXR) agonist. FXR activation suppresses de novo synthesis of bile acids in hepatocytes as well as increases the transport of bile acids out of hepatocytes, thereby reducing exposure of the hepatocytes to bile acid. It is indicated for primary biliary cholangitis (PBC) in combination with ursodeoxycholic acid (UDCA) in adults with an inadequate response to UDCA for at least 1 y or as monotherapy in adults unable to tolerate UDCA.



Class Summary

Alleviation of itching associated with excessive bile acid levels.

Cholestyramine (Questran)

Forms a nonabsorbable complex with bile acids in the intestine, which in turn inhibits the enterohepatic reuptake of intestinal bile salts.

Rifampin (Rifadin)

Antimycobacterial agent noted to alleviate pruritus in 79% of patients with primary biliary cholangitis. This effect may be a result of changed metabolism of liver bile acids or by altered bacterial metabolism by intestinal bacteria.

Naloxone (Narcan)

Opioid antagonist useful in the treatment of pruritus.