Ion exchange mechanism of bile acid sequestrants in preventing reabsorption of bile salts in hypercholesterolemia

Abstract

Hypercholesterolemia is the presence of high levels of cholesterol in the blood. It is a form of "hyperlipidemia" (elevated levels of lipids in the blood) and "hyperlipoproteinemia" (elevated levels of lipoproteins in the blood). Cholesterol is a sterol. It is one of three major classes of lipids which all animal cells utilize to construct their membranes and is thus manufactured by all animal cells. Plant cells do not manufacture cholesterol. It is also the precursor of the steroid hormones, bile acids and vitamin D. Since cholesterol is insoluble in water, it is transported in the blood plasma within protein particles (lipoproteins). Lipoproteins are classified by their density: very low density lipoprotein (VLDL), intermediate density lipoprotein (IDL), low density lipoprotein (LDL) and high density lipoprotein (HDL). All the lipoproteins carry cholesterol, but elevated levels of the lipoproteins other than HDL (termed non-HDL cholesterol), particularly LDL-cholesterol are associated with an increased risk of atherosclerosis and coronary heart disease. In contrast, higher levels of HDL cholesterol are protective. Elevated levels of non-HDL cholesterol and LDL in the blood may be a consequence of diet, obesity, inherited (genetic) diseases (such as LDL receptor mutations in familial hypercholesterolemia), or the presence of other diseases such as diabetes and an underactive thyroid. Reducing saturated dietary fat is recommended to reduce total blood cholesterol and LDL in adults. In people with very high cholesterol (e.g. familial hypercholesterolemia), diet is often insufficient to achieve the desired lowering of LDL and lipid lowering medications which reduce cholesterol production or absorption are usually required. If necessary, other treatments such as LDL aphaeresis or even surgery (for particularly severe subtypes of familial hypercholesterolemia) are performed.