Chenodiol (Chenodeoxycholic Acid)
- Atc Codes:A05AA01
- CAS Codes:99102-69-9
- PHARMGKB ID:99102-69-9
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Germany: Xenbilox; Poland: Chenofalk; Portugal: Xebyl.
North America
USA: Chenodiol.
Asia
Japan: Chenix.
Drug combinations
Chenodiol and Ursodeoxycholic Acid
Chemistry
Chenodiol: C~24~H~40~O~4~. Mw: 392.58. (1)(4R)-4-[(3R,5S,7R,8R,9S,10S,13R,14S,17R)-3,7-dihydroxy-10,13-dimethyl-2, 3,4,5,6,7,8,9,11,12,14,15,16; (2) 3α, 7α-dihydroxy-5β-cholan-24-oic acid. CAS: 99102-69-9.
Pharmacologic Category
Cholelitholytic Agents; Human Bile Acid. (ATC-Code: A05AA01).
Mechanism of action
Chenodiol suppresses hepatic synthesis of both cholesterol and cholic acid, gradually replacing the latter and its metabolite, deoxycholic acid, in an expanded bile acid pool. These actions contribute to biliary cholesterol desaturation and gradual dissolution of radiolucent cholesterol gallstones in the presence of a gall-bladder visualized by oral cholecystography. Chenodiol has no effect on radiopaque (calcified) gallstones or on radiolucent bile pigment stones.
Therapeutic use
Indicated for patients with radiolucent stones in well-opacifying gallbladders, in whom selective surgery would be undertaken except for the presence of increased surgical risk due to systemic disease or age.
Pregnancy and lactiation implications
Chenodiol is contraindicated in women who are or may become pregnant. Caution should be exercised when administered to nursing women.
Unlabeled use
Contraindications
Presence of known hepatocyte dysfunction or bile ductal abnormalities such as intrahepatic cholestasis, primary biliary cirrhosis or sclerosing cholangitits. A gallbladder confirmed as nonvisualizing after two consecutive single doses of dye. Radiopaque stones, gallstone complications or compelling reasons for gallbladder surgery including unremitting acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, or biliary gastrointestinal fistula.
Warnings and precautions
Safe use of chenodiol depends upon selection of patients without pre-existing liver disease and upon faithful monitoring of serum aminotransferase levels to detect drug-induced liver toxicity. Aminotransferase elevations over three times the upper limit of normal have required discontinuation of chenodiol (2%-3%). Epidemiologic studies suggest that bile acids might contribute to human colon cancer, but direct evidence is lacking.