Published online Nov 15, 2010. doi: 10.4239/wjd.v1.i5.146
Revised: August 27, 2010
Accepted: September 3, 2010
Published online: November 15, 2010
Cholestyramine is a first-generation bile acid sequestrant (BAS) and antihyperlipidemic agent that currently has limited use because of its relatively weak effect on lowering low density-lipoprotein (LDL)-cholesterol (C) and poor tolerability. The current first choice drugs for hyper-LDL-cholesterolemia are 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors (statins) because of their strong LDL-C lowering effects and efficacy in prevention of cardiovascular disease. However, after lowering the target levels of LDL-C in very high risk patients, combination therapy with statins and other antihyperlipidemic drugs may become more important for treatment of hyper-LDL-cholesterolemia. Second-generation BASs such as colesevelam and colestimide have a glucose-lowering effect and improved tolerance, which has led to re-evaluation of their utility in combination with statins or antidiabetic agents.