Gallstone Dissolution Agent
Gallbladder stone dissolution
Not to be used with cholesterol, radiopaque, bile pigment stones, or stones
>20 mm in diameter; allergy to bile acids
Gallbladder stone dissolution may take several months of therapy; complete
dissolution may not occur and recurrence of stones within 5 years has been
observed in 50% of patients; use with caution in patients with a nonvisualizing
gallbladder and those with chronic liver disease; not recommended for
1% to 10%: Gastrointestinal: Diarrhea
<1%: Fatigue, headache, pruritus, rash, nausea, vomiting, dyspepsia,
metallic taste, abdominal pain, biliary pain, constipation
Symptoms of overdose include diarrhea
No specific therapy for diarrhea and for overdose
Decreased effect with aluminum-containing antacids, cholestyramine,
colestipol, clofibrate, oral contraceptives (estrogens)
Do not store above 30°C
Decreases the cholesterol content of bile and bile stones by reducing the
secretion of cholesterol from the liver and the fractional reabsorption of
cholesterol by the intestines
Metabolism: Undergoes extensive enterohepatic recycling; following hepatic
conjugation and biliary secretion, the drug is hydrolyzed to active ursodiol,
where it is recycled or transformed to lithocholic acid by colonic microbial
Half-life: 100 hours
Elimination: In feces via bile
Adults: Oral: 8-10 mg/kg/day in 2-3 divided doses; use beyond 24 months is
not established; obtain ultrasound images at 6-month intervals for the first
year of therapy; 30% of patients have stone recurrence after
ALT, AST, sonogram
|Mental Health: Effects
on Mental Status|
May cause drowsiness
Effects on Psychiatric
|Dental Health: Local
No information available to require special precautions
Effects on Dental Treatment|
No effects or complications reported
Frequent blood work will be necessary to follow drug effects. Drug will need
to be taken for 1-3 months after stone is dissolved. Stones may recur. Report
any persistent nausea, vomiting, abdominal pain, or yellowing of skin or eyes.
Breast-feeding precautions: Consult prescriber if
Capsule: 300 mg
A 60 mg/mL ursodiol suspension may be made by opening twelve 300 mg capsules
and wetting with sufficient glycerin and triturating to make a fine paste;
gradually add 45 mL of simple syrup in three steps:
2. Rinse mortar with 10 mL simple syrup and add to amber bottle
3. Repeat step 2 with sufficient syrup to make 60 mL final volume; label
"Shake Well and Store in Refrigerator"; 35-day stability
Colombo C, Setchell KD, Podda M, et al,
"Effect of Ursodeoxycholic Acid Therapy for Liver Disease Associated With Cystic Fibrosis,"
J Pediatr, 1990, 117(3):482-9.
Johnson CE and Nesbitt J,
"Stability of Ursodiol in an Extemporaneously Compounded Oral Liquid," Am J
Health Syst Pharm, 1995, 52(16):1798-800.
Lepage G, Paradis K, Lacaille F, et al,
"Ursodeoxycholic Acid Improves the Hepatic Metabolism of Essential Fatty Acids and Retinol in Children With Cystic Fibrosis,"
J Pediatr, 1997, 130(1)52-8.
Spagnuolo MI, Iorio R, Vegnente A, et al,
"Ursodeoxycholic Acid for Treatment of Cholestasis in Children on Long-Term Total Parenteral Nutrition - A Pilot Study,"
Gastroenterology, 1996, 111(3):716-9.
Ullrich D, Rating D, Schroter W, et al,
"Treatment With Ursodeoxycholic Acid Renders Children With Biliary Atresia Suitable for Liver Transplantation,"
Lancet, 1987, 2(8571):1324.
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