Review
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World J Diabetes. Nov 15, 2010; 1(5): 146-152
Published online Nov 15, 2010. doi: 10.4239/wjd.v1.i5.146
Role of bile acid sequestrants in the treatment of type 2 diabetes
Kohzo Takebayashi, Yoshimasa Aso, Toshihiko Inukai
Kohzo Takebayashi, Yoshimasa Aso, Toshihiko Inukai, Department of Internal Medicine, Dokkyo Medical University Koshigaya Hospital, Koshigaya 343-8555, Japan
Author contributions: Takebayashi K wrote this manuscript; and Aso Y and Inukai T reviewed the manuscript.
Correspondence to: Kohzo Takebayashi, MD, Department of Internal Medicine, Dokkyo Medical University Koshigaya Hospital, 2-1-50, Minami-Koshigaya, Koshigaya, Saitama 343-8555, Japan. takeb@gmail.plala.or.jp
Telephone: +81-48-9651111 Fax: +81-48-9651127
Received: June 22, 2010
Revised: August 27, 2010
Accepted: September 3, 2010
Published online: November 15, 2010
Abstract

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.

Keywords: Bile acid, Bile acid sequestrant, Type 2 diabetes