No

Gallstone Dissolution Agent

Gallbladder stone dissolution

B

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 children

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 (86°F)

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 flora

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 dissolution

ALT, AST, sonogram

May cause drowsiness

None reported

No information available to require special precautions

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 breast-feeding.

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.