Significance of LDL-C Lowering Therapy in Diabetic Patients

Sergio Martinez-Hervas; Rafael Carmena; Juan F Ascaso


Clin Lipidology. 2011;6(4):389-399. 

In This Article

Bile Acid Sequestrants (Resins)

Bile acid sequestrants are nonsoluble polymers that trap bile acids in the intestinal lumen and promote their excretion in feces. As a consequence, they lower the hepatic cholesterol pool and promote the expression of LDL receptors in the liver. Bile acid sequestrants are the safest lipid-lowering drugs but have frequent undesirable gastrointestinal effects. In lipid-lowering trials, bile acid sequestrants, such as colesevelam, cholestyramine, colestipol, and colestimide, at maximum dose, lower LDL-C by 15–21%, and raise HDL-C by 3–9% and TG by 2–16%.[72] Bile acid sequestrants are used in the treatment of hypercholesterolemia, in monotherapy when statins are not well tolerated or in combination with statins when statins alone are not able to achieve the LDL-C target.

Cholestyramine and colestipol have demonstrated to be efficient in the lowering of LDL-C and reducing coronary death. In the Lipid Research Clinics Coronary Primary Prevention Trial (LRC-CPPT) cholestyramine reduced CHD risk and decreased LDL-C by 12%.[73]

The second generation of bile acid sequestrants, for example colesevelam, is more specific, binds bile acids with greater affinity and is better tolerated. As monotherapy at a daily dose of 3.8 g colesevelam reduces LDL-C by up to 16% in hypercholesterolemic patients. An additive effect in combination with atorvastatin and simvastatin has been observed.[74,75] Moreover, an important action of the bile acid sequestrants is the lowering of plasma glucose and glycosylated hemoglobin levels in an important way (0.9%).[76] Thus, they are useful in the treatment of hypercholesterolemia in diabetes.


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