Pharm

Bile Acid Oral Dissolution Therapy

Bile Acid Oral Dissolution Therapy, Ursodeoxycholic Acid, Ursodiol, Actigal, Chenodeoxycholic Acid, Oral Dissolution Therapy, Gallstone Dissolving Agent

Mechanism

Bile Acid Oral Dissolution Therapy in general
1. Decreases biliary Cholesterol hepatic secretion
2. Forms unsaturated bile
3. Promotes dissolution of Cholesterol crystals and Gallstones
Ursodeoxycholic Acid (UDCA, Ursodiol)
1. Naturally occurring hydrophilic bile acid
2. Protects bile ducts by detoxifying hydrophobic bile acids
3. Decreases cholic acid and increases Chenodeoxycholic Acid levels
  1. Reverses the effects of Intrahepatic Cholestasis of Pregnancy

Indications

Intrahepatic Cholestasis of Pregnancy (Ursodeoxycholic Acid only)
Cholelithiasis
1. Comorbid condition that precludes safe Cholecystectomy and Symptomatic Gallstones
2. Symptomatic patient unwilling to undergo surgery
  1. Small Gallstones (<5mm) with functioning gallbladder and no cystic duct obstruction

Contraindications

Excludes the 85% of patients who cannot meet the following criteria
1. Gallstones >0.5mm (as opposed to the normal small, floating, Cholesterol Gallstones)
2. Non-functional Gallbladder

Dosing
Ursodiol or Ursodeoxycholic Acid (UDCA, Actigal)

Dose: 8-15 mg/kg/day or 500 mg orally twice daily
Course: 6-12 months (in Symptomatic Gallstones) or until delivery in Intrahepatic Cholestasis of Pregnancy

Dosing
Chenodeoxycholic Acid

Do NOT use in pregnancy (Pregnancy Category X)
Start: 250 mg twice daily for 2 weeks
Titrate
1. Increase by 250 mg/day each week
2. Maximum: 13-16 mg/kg/day divided bid (or until sub-maximal dose that is tolerated)

Efficacy
Cholelithiasis

Stones dissolving over 6-12 months: 60-90%
Stones reoccuring within 5 years: 25-50%
Better prognosis associated factors
1. Single Gallstone AND
2. Non-obese AND
3. Young patient

References