Bile Acid Sequestrants
Bile acids have long been considered as nothing more than emulsifiers of lipids. As such, bile acids could excite few hepatologists. However, it now appears that bile acids have important and intriguing signalling functions - Peter L.M. Jansen
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Diabetes Medicine: Bile Acid Sequestrants and Dopamine Receptor Agonists
Bile acid sequestrants are a type of medicine that is mostly used to lower LDL (“bad”) cholesterol. As the name suggests, these medicines bind to bile acids in the intestines and prevent them from being absorbed back into the blood. The liver then makes more bile; cholesterol is used to make bile, so more cholesterol is used by the liver, thus reducing the amount of cholesterol in the blood. While statins are more commonly used these days to help lower cholesterol, not everyone can take them, so bile acid sequestrants are another option.
One of the drugs in this class is called colesevelam (brand name Welchol). Not only does it lower LDL cholesterol, it lowers blood sugar, too, when…
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A new life for bile acids
Bile acids have long been considered as nothing more than emulsifiers of lipids. As such, bile acids could excite few hepatologists. However, it now appears that bile acids have important and intriguing signalling functions and researchers from many corners including the industry have come to see what is going on.
Articles of Interest
Bile acid sequestrants in type 2 diabetes: potential effects on GLP1 secretion
In recent years, it has become clear that bile acids are candidate agents in newly identified pathways through which carbohydrate metabolism and lipid metabolism are regulated.
Bile Acid Sequestrants for Lipid and Glucose Control
Bile acid sequestrants have also been shown to improve glycemic control in patients with type 2 diabetes mellitus (T2DM). In initial studies in patients with T2DM and dyslipidemia, cholestyramine therapy decreased LDLC levels by 28% and resulted in improved glycemic control, as defined by a 13% reduction in mean plasma glucose levels, a median reduction of 0.22 g/d in urinary glucose excretion, and a tendency toward a lower concentration of glycosylated hemoglobin A1c (HbA1c).
Bile acids in glucose metabolism in health and disease
The knowledge gained from observations in mice and humans enhances our understanding that some BAs may play important roles in regulating the glycemic response in health and in T2DM.
Intestinal bile acid receptors are key regulators of glucose homeostasis
Although some discrepancies remain on the overall role of the bile acid receptors TGR5 and FXR in glucose metabolism, recent studies clearly highlight that these receptors in the intestine seems to be crucial to maintain glucose homeostasis.
Role of Bile Acid Sequestrants in the Treatment of Type 2 Diabetes
In addition to significant lipid-lowering properties, data from several studies suggest that BASs might also improve glycemic control in patients with type 2 diabetes.
Resources
GoodRx
Bile acid sequestrants are used to lower cholesterol levels to treat high cholesterol. They work by removing bile acids from the body.
Welchol
Welchol, along with diet and exercise, is the only FDA-approved medicine with a single active ingredient proven to lower both high blood sugar (A1C) and LDL-C or “bad” cholesterol in adults with type 2 diabetes and high cholesterol.
ScienceDirect
Bile acid sequestrants reduce the reabsorption of secreted bile acids, eventually reducing serum cholesterol levels by increasing the conversion of hepatic cholesterol to bile acids, thus reducing the cholesterol content of the hepatocytes.
