Much progress has been made during the past two decades in the management of lipid disorders and consequent reduction in mortality from cardiovascular disease. However, many people remain inadequately treated and not at lipid goals. Bile acid sequestrants (BAS) have been an effective modality for treatment of hypercholesterolemia and elevated low-density lipoprotein-cholesterol (LDL-C) for more than 50 years. Well- designed angiographic and clinical trials have documented the successful reduction in atherosclerotic burden and cardiovascular events with the use of BAS in monotherapy and combination therapy with other lipid-lowering agents. Despite the availability of statins as the preferred agents for LDL-C lowering, BAS have proven to be of value as second-line therapy or as adjunct therapy when LDL-C goals are not achievable with statins alone. Due to a lack of systemic absorption, BAS have no major adverse effect. The newer BAS may be associated with better tolerability and side effects. In patients with type 2 diabetes, or those at a risk of diabetes, BAS have a unique advantage of a dual effect, namely reduction in LDL-C and a modest but significant effect on reducing hyperglycemia. The precise mechanism of the glucose-lowering effect is not fully understood.
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