Interrupting bile-acid handling and lipid and glucose control: Effects of colesevelam on glucose levels

The digestive tract plays a key role in lipid metabolism and in cardiovascular risk through the physiology of bile acids on lipid absorption, enterohepatic recycling of bile acids, and cholesterol oxidation in synthesis of bile acids. Recent evidence associates the activation of farnesoid X receptor by bile acids with alterations in high-density lipoprotein cholesterol, triglyceride metabolism, and glucose metabolism. Bile-acid sequestrants augment cholesterol excretion via enhanced conversion to bile acids to lower low-density lipoprotein cholesterol. Several recent studies have demonstrated a role for the bile-acid sequestrant colesevelam hydrochloride in improving glycemic control as well as lipid profiles in subjects with type 2 diabetes. This work reviews the mechanisms of action of colesevelam hydrochloride in interrupting bile acid reabsorption and in lipid transport and glucose control.