No

Bile Acid

Oral dissolution of cholesterol gallstones in selected patients

X

Presence of known hepatocyte dysfunction or bile ductal abnormalities; a gallbladder confirmed as nonvisualizing after two consecutive single doses of dye; radiopaque stones; gallstone complications or compelling reasons for gallbladder surgery; inflammatory bowel disease or active gastric or duodenal ulcer; pregnancy

Chenodiol is hepatotoxic in animal models including subhuman Primates; chenodiol should be discontinued if aminotransferases exceed 3 times the upper normal limit; chenodiol may contribute to colon cancer in otherwise susceptible individuals

>10%:

Gastrointestinal: Diarrhea (mild), biliary pain

Miscellaneous: Aminotransferase increases

1% to 10%:

Endocrine & metabolic: Increases in cholesterol and LDL cholesterol

Gastrointestinal: Dyspepsia

<1%: Diarrhea (severe), cramps, nausea, vomiting, flatulence, constipation, leukopenia, intrahepatic cholestasis, higher cholecystectomy rates

Symptoms of overdose may include diarrhea; a rise in liver function tests has been observed

No specific antidote, institute supportive therapy

Decreased effect: Antacids, cholestyramine, colestipol, oral contraceptives

Chenodiol is a primary acid excreted into bile, normally constituting one-third of the total biliary bile acids. Synthesis of chenodiol is regulated by the relative composition and flux of cholesterol and bile acids through the hepatocyte by a negative feedback effect on the rate-limiting enzymes for synthesis of cholesterol (HMG CoA reductase) and bile acids (cholesterol 7 alpha-hydroxyl).

Adults: Oral: 13-16 mg/kg/day in 2 divided doses, starting with 250 mg twice daily the first 2 weeks and increasing by 250 mg/day each week thereafter until the recommended or maximum tolerated dose is achieved

Oral cholecystograms and/or ultrasonograms should be used to monitor response; dissolutions of stones should be confirmed 1-3 months later

aminotransferases, cholesterol, LDL cholesterol, triglycerides, bilirubin (I)

None reported

May rarely produce leukopenia; use caution with clozapine and carbamazepine

No information available to require special precautions

No effects or complications reported

Take as directed, for entire length of therapy. Medication may need to be taken for 24 months before dissolution will occur. Avoid aluminum-based antacids during entire course of therapy. Blood studies and x-rays studies will be necessary during therapy. Report persistent diarrhea and gallstone attacks (abdominal pain, nausea and vomiting, yellowing of skin or eyes). Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant and do not get pregnant during or for 1 month following therapy. Consult prescriber for instruction on appropriate contraceptive measures. This drug may cause severe fetal defects. Do not donate blood during or for 1 month following therapy. Breast-feeding is not recommended.

Tablet, film coated: 250 mg