Oxygenated derivatives of cholesterol (oxysterols) present a remarkably diverse profile of biological activities, including effects on sphingolipid metabolism, platelet aggregation, apoptosis, and ...

Oxysterols: modulators of cholesterol metabolism and other processes.

Quantitative estimation of the hydrophilic-hydrophobic balance of mixed bile salt solutions.

A double-masked study was conducted to determine the efficacy and safety of randomly allocated chenodiol (chenodeoxycholic acid, 750 mg/d or 350 mg/d) or placebo administered for 2 years t...

Chenodiol (Chenodeoxycholic Acid) for Dissolution of Gallstones: The National Cooperative Gallstone Study

The pharmacokinetics, metabolism, as well as the pharmacodynamic actions of ursodeoxycholic acid are reviewed and related to its physicochemical properties. Ursodeoxycholic acid is absorbed incompletely because of its low aqueous solubility. After absorption, it is conjugated with glycine or taurine and circulates with the endogenous bile acids. At usual doses (8-10 mg/kg/day), the pool of ursodeoxycholyl conjugates constitutes 30-60% of circulating bile acids. Ursodeoxycholic acid is metabolized by intestinal bacteriae to lithocholic acid which does not accumulate in the circulating bile acids because of efficient hepatic sulfation. Administration of ursodeoxycholic acid causes decreased cholesterol absorption, increased bile acid biosynthesis, and decreased biliary cholesterol secretion. Ursodeoxycholic acid is a choleretic agent, as all bile acids, but differs from other dihydroxy-bile acids in being non-cytotoxic because it has less affinity for membranes, and when present at micellar concentrations does not solubilize membranes. Chronic administration of ursodeoxycholic acid appears to increase canalicular transport.

Pharmacology of ursodeoxycholic acid, an enterohepatic drug.

Ursodeoxycholic acid is the 7 beta-hydroxy epimer of chenodeoxycholic acid and is normally present in only trace amounts in the bile. Oral administration of pharmacological doses markedly decreases biliary cholesterol saturation. Complete or partial dissolution of radiolucent gallstones located in a functioning gallbladder occurred in about 40 to 55% of patients treated with ursodeoxycholic acid in controlled studies of 6 months duration. Patients showing partial gallstone dissolution at that time are likely to continue improving possibly to complete gallstone dissolution with continued therapy. The success rate with ursodeoxycholic acid may be increased top about 80% if more stringent patient selection criteria are applied to include only those with non-calcified floating cholesterol stones of less than 10 to 15 mm diameter. Those with calcified stones or stones greater than 15 mm diameter or unlikely to respond to ursodeoxycholic acid therapy. The optimal dose in published studies was about 8 to 10 mg/kg/day, which is about half to two-thirds the dose of chenodeoxycholic acid (15 mg/kg/day) achieving approximately equivalent results. Ursodeoxycholic acid appears to be remarkably well tolerated, with diarrhoea occurring in only a very small proportion of patients. While surgery is clearly the preferred treatment in many patients with symptomatic gallstones, in a carefully selected subgroup of such patients gallstone dissolution therapy with ursodeoxycholic acid offers an important and worthwhile alternative.

Ursodeoxycholic acid: a review of its pharmacological properties and therapeutic efficacy

Hepatic cholesterol and bile acid metabolism in subjects with gallstones: comparative effects of short erm feeding of chenodeoxycholic and ursodeoxycholic acid.

Medical treatment of radiolucent gallstones with chenodeoxycholic acid (CDCA) a follow-up report at four years.

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Hepatic cholesterol and bile acid metabolism in subjects with gallstones: comparative effects of short erm feeding of chenodeoxycholic and ursodeoxycholic acid.

Medical treatment of radiolucent gallstones with chenodeoxycholic acid (CDCA) a follow-up report at four years.