ursodiol

Warnings
Contraindications
Hypersensitivity
Gallstone complication requiring surgery
Known hepatocyte or bile ductal abnormalities, inflammatory bowel disease
Calcified gallstones, bile acid allergy, chronic hepatic disease
Billiary gastrointestinal fistula
Patients requiring cholecystectomy
Adverse Effects
>10%
Headache
Dizziness
Diarrhea
Dyspepsia
Nausea/vomiting
Back pain
Upper respiratory tract infection
1-10%
Alopecia
Rash
Hyperglycemia
Flatulence
Peptic ulcer
Urinary tract infection
Leukopenia
Thrombocytopenia
Cholecystitis
>1%
Fatigue
Abdominal pain
Thrombocytopenia
Pruritus
Angioedema
Peripheral edema
Biliary pain
Postmarketing Reports
Hepatobiliary disorders: Jaundice (or aggravation of pre-existing jaundice)
Abnormal laboratory tests: Increased ALT, AST, alkaline phosphatase, bilirubin, gamma-GT
Pharmacology
Mechanism of Action
Naturally-occurring bile acid; reduces cholesterol secretion from the liver; reduces the fractional
reabsorption of cholesterol by the intestines.
Absorption
Bioavailability: 90%
Onset: Initial response for gallstone dissolution is 3-6 months
Distribution
Protein Bound: 70%
Metabolism
Taken up rapidly by the liver, conjugated with glycine or taurine, and excreted in the bile
Nonabsorbed ursodiol passes into the colon where it is 7-dehydroxylated to lithocholic acid (an
intermediary compound, sometimes formed, is called chenodiol); chenodiol is then dehydroxylated
to lithocholic acid
Metabolites: Glyco-ursodeoxycholic acid, tauro-ursodeoxycholic acid, 7-keto-lithocholic acid
(inactive); lithocholic acid (inactive) is formed from the 7-hydroxylation of ursodiol and chenodiol;
a small portion is metabolized to sulfated lithocholic acid conjugates which are excreted in bile &
eliminated in feces
Elimination
Excretion: Mainly in feces