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Bile acid sequestrants

Bile acid sequestrants belong to the pharmaceutical API subcategory of cholesterol-lowering agents. These agents are primarily used in the management of hypercholesterolemia and related cardiovascular conditions. Bile acid sequestrants function by binding to bile acids in the gastrointestinal tract, forming a complex that prevents their reabsorption. This mechanism promotes the excretion of bile acids in the feces and subsequently increases the hepatic conversion of cholesterol to bile acids, leading to a reduction in circulating cholesterol levels.

Bile acid sequestrants are commonly prescribed as adjunct therapy to statins or as an alternative for individuals who cannot tolerate statin therapy. They are typically administered orally in the form of powders, tablets, or granules, and they are not absorbed into the bloodstream. This characteristic makes them relatively safe, with a low risk of systemic side effects.

The main bile acid sequestrants used in clinical practice include cholestyramine, colesevelam, and colestipol. These agents have demonstrated efficacy in reducing low-density lipoprotein cholesterol (LDL-C) levels and improving lipid profiles. Additionally, they may have secondary benefits, such as improving glycemic control in patients with type 2 diabetes and reducing the risk of cardiovascular events.

Overall, bile acid sequestrants play a vital role in managing hypercholesterolemia and are an important component of cardiovascular disease management. With their cholesterol-lowering properties and favorable safety profile, they offer an effective therapeutic option for patients seeking to improve their lipid profiles and reduce their risk of cardiovascular complications.