Cholesterol Lowering Drugs

Drug Class

Examples

Mechanism of Action

Expected Effect

Side Effects

Statins (HMG-CoA Reductase Inhibitors)

Atorvastatin (Lipitor), Simvastatin, Rosuvastatin

Inhibit HMG-CoA reductase, reducing cholesterol synthesis in the liver

Lower LDL & total cholesterol, increase HDL

Muscle pain (myopathy), liver toxicity, rhabdomyolysis

Bile Acid Sequestrants

Cholestyramine, Colesevelam

Bind bile acids in the intestines, forcing the liver to use cholesterol to make more bile

Lower LDL cholesterol

GI issues (constipation, bloating), vitamin deficiency (A, D, E, K)

Fibrates (Fibric Acid Derivatives)

Gemfibrozil, Fenofibrate

Activate lipoprotein lipase, increasing breakdown of triglycerides

Lower triglycerides, increase HDL

Gallstones, liver toxicity, myopathy (especially with statins)

Niacin (Vitamin B3)

Nicotinic Acid

Decreases liver production of LDL & triglycerides, increases HDL

Lower LDL & triglycerides, increase HDL

Flushing, liver toxicity, hyperglycemia

Cholesterol Absorption Inhibitors

Ezetimibe (Zetia)

Blocks cholesterol absorption in the intestines

Lower LDL cholesterol

GI upset, liver toxicity (when combined with statins)

PCSK9 Inhibitors

Alirocumab, Evolocumab

Block PCSK9 enzyme, increasing LDL receptor availability

Lower LDL cholesterol (especially in high-risk patients)

Injection site reactions, flu-like symptoms

Omega-3 Fatty Acids

Lovaza, Vascepa

Reduce liver production of triglycerides

Lower triglycerides

Fishy taste, bleeding risk (high doses)