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  • Cholesterol: Metabolism and excretion Cholesterol is oxidized by the liver into a variety of bile acids. These in turn are conjugated with glycine, taurine, glucuronic acid, or sulfate. A mixture of conjugated and non-conjugated bile acids along with cholesterol itself is excreted from the liver into the bile. Approximately 95% of the bile acids are reabsorbed from the intestines and the remainder lost in the feces. The excretion and reabsorption of bile acids forms the basis of the enterohepatic circulation which is essential for the digestion and absorption of dietary fats. Under certain circumstances, when more concentrated, as in the gallbladder, cholesterol crystallises and is the major constituent of most gallstones, although lecithin and bilirubin gallstones also occur less frequently.

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  • Clinical Trials - Pharmacology - Excretion - Biliary Excretion - Merck Manual Professional - 2007: Biliary excretion: Some drugs and their metabolites are extensively excreted in bile. Because they are transported across the biliary epithelium against a concentration gradient, active secretory transport is required. When plasma drug concentrations are high, secretory transport may approach an upper limit (transport maximum). Substances with similar physicochemica l properties may compete for excretion. Drugs with a mol wt > 300 g/mole and with both polar and lipophilic groups are more likely to be excreted in bile; smaller molecules are generally excreted only in negligible amounts. Conjugation, particularly with glucuronic acid, facilitates biliary excretion. In the enterohepatic cycle, a drug secreted in bile is reabsorbed into the circulation from the intestine. Biliary excretion eliminates substances from the body only to the extent that enterohepatic cycling is incomplete?whe n some of the secreted drug is not reabsorbed from the intestine.

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