Ursodiol

Generic Name: Ursodiol
Common Brand Names: Actigall, Urso 250, Urso Forte

Introduction

Ursodiol (also known as ursodeoxycholic acid) is a bile acid used to treat certain types of liver disease, particularly primary biliary cholangitis (PBC) and to dissolve cholesterol gallstones. It works by decreasing the amount of cholesterol produced by the liver and by improving bile flow.

Conditions of Use (Indications)

  1. Primary Biliary Cholangitis (PBC): Used to slow the progression of PBC by improving bile flow and reducing liver damage.
  2. Cholesterol Gallstones: Helps dissolve cholesterol-containing gallstones, particularly in patients who are not candidates for gallbladder surgery.
  3. Cystic Fibrosis-Related Liver Disease: Occasionally used in patients with cystic fibrosis to improve liver function.
  4. Non-Alcoholic Fatty Liver Disease (NAFLD): Used off-label to improve liver function in patients with NAFLD.

Mechanism of Action

Ursodiol is a naturally occurring bile acid that works by decreasing the hepatic secretion of cholesterol into bile. It reduces the cholesterol content of bile, preventing the formation of gallstones and promoting the dissolution of existing cholesterol gallstones. Additionally, it helps to decrease bile acid toxicity to liver cells, providing protection to the liver in conditions like PBC.

Side Effects

1.Common:

  • Diarrhea, nausea, and abdominal discomfort.

2.Serious:

  • Liver enzyme abnormalities, which may require discontinuation of the drug.
  • Severe allergic reactions (rare).

Harmful Interactions

  1. Cholestyramine: May reduce the effectiveness of ursodiol by binding to it in the gastrointestinal tract.
  2. Cyclosporine: Ursodiol may increase the levels of cyclosporine, leading to increased risk of toxicity.
  3. Estrogens: Estrogen therapy may increase the cholesterol content of bile, reducing the effectiveness of ursodiol.

Contraindications

  1. Hypersensitivity to ursodiol or any component of the formulation.
  2. Acute liver disease (e.g., hepatitis) or cirrhosis with decompensated liver function.
  3. Pregnancy and breastfeeding (unless clearly needed, with caution).

Latest References

  1. Mayo Clinic. (2023). “Ursodiol: Clinical Uses and Efficacy in Primary Biliary Cholangitis.” Mayo Clinic Proceedings, DOI: 10.1016/j.mayocp.2023.03.011.
  2. National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK). (2022). “Ursodeoxycholic Acid and Gallstone Treatment.” NIDDK Publications.