Cholestyramine resin is a bile acid sequestrant that reduces low-density-lipoprotein cholesterol (LDL-c) through partial interruption of enterohepatic bile acid circulation. This drug has no systemic effects and consequently can be used in women of reproductive age, in children and in patients with muscular, liver or renal disorders. Cholestyramine resin should be administered separately from other drugs. This agent boosts the lipidlowering effect of statins, as well as that of fibrates, nicotinic acid and ezetimibe. Adding cholestyramine resin to statin therapy reduces LDL-c by an additional 20%, equivalent to a 3-fold increase in the statin dose. A meta-analysis of eight clinical trials found that resins reduced mortality from cardiac causes by 30%(OR 0.70; 95%CI 0.50-0.99), a figure not lower than that observed with statins. Cholestyramine resin reduces postprandial glycemia and glycosylated hemoglobin and consequently is of particular interest in the treatment of hypercholesterolemia in patients with metabolic syndrome or type 2 diabetes who have failed to achieve LDL-c targets with statin monotherapy. Previously used resin preparations often produced gastrointestinal intolerance, while the new galenical preparations of cholestyramine resin used at a dose of 4-8 grams (1-2 sachets) per day - sufficient to obtain a lipid-lowering effect - are usually well tolerated.