Bile Acid Sequesters

One of the ways in which cholesterol is catabolized in the organism is by its transformation into bile acids, the most important of which are cholic, deoxycholic, lithocholic, and cholanic acids.

deoxycholic acid lithocholic acid cholanic acid

Binding of bile acids and their removal from the organism disturbs the balance of cholesterol and bile acids, and a compensatory increase of the transformation of cholesterol into deoxycholic acid lithocholic acid cholanic acid

Binding of bile acids and their removal from the organism disturbs the balance of cholesterol and bile acids, and a compensatory increase of the transformation of cholesterol into bile acids begins, which results in a decreased content of cholesterol. Drugs that remove cholesterol in the form of insoluble bile acid derivatives stimulate transformation of cholesterol into bile acids by the organism. The resulting effect is an overall reduction in the amount of cholesterol in the organism.

Currently, there are two drugs that bind with the gastric tract and release bile acids from the organism—colestipol and cholestyrolramine. Both are macromolecular compounds— anion-exchange resins. They differ from one another in that they have different chemical structures; however, they have the same mechanism of action. Being insoluble in water, they are not absorbed from the gastrointestinal tract and bind with bile acids at their quaternary ammonium regions, where they are removed with feces in the form of an ionexchange resin to which they are bound.

Colestipol: Colestipol (20.1.1) is a hydrochloride of the product of copolymerization of epichlorohydrine with diethylentriamine that contains varying numbers of quaternary nitrogen atoms. There is no exact formula of the product of copolymerization, but its approximate structure can be expressed as 20.1.1 [1-4].

—(NH—CH2-CH2-NH-CH2-CH2-NH-CH2-CH-CH2 —N^CH2-CH2-NH-CH2-CH2-NH-^ ' mHCI

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