Drugs that Regulate Lipoprotein Metabolism

Lipoproteins, differentiated on the basis of density, size, and protein content, are essential for the biogenesis of plasma membrane and maintenance of its integrity; they also serve as sources of energy, hormone precursors, and signaling molecules.³ In blood, lipoproteins transport cholesterol and triglycerides. Abnormalities of lipoprotein metabolism appear to be the result of genetic factors, which modify the sensitivity of individuals to adverse dietary habits and to sedentary lifestyles.

Elevated cholesterol-rich low-density lipoproteins (LDLs) and lipoproteins that are rich in triglycerides (TGs), and decreased levels of high-density lipoproteins (HDLs) are strongly associated with atherosclerosis.³ Diet and exercise can reduce total plasma cholesterol concentrations by as much as 25%. If this approach is insufficient to normalize lipid levels drug therapy is initiated. Drugs in the top 300 that regulate lipoprotein metabolism (Table 1) fall into six major classes.^2,3,10

Table 1. Drugs that Affect Cholesterol and Lipoprotein Metabolism.^2,^3,¹⁰

Drugs	Mechanisms of Action	Common Indications
Inhibitors of cholesterol synthesis Atorvastatin Simvastatin Pravastatin Rosuvastatin Lovastatin	Inhibit HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis Decrease LDL Decrease TG Increase HDL	Hypercholesterolemia Prophylaxis for coronary atherosclerosis
Inhibitors of bile acid absorption Colestipol	Bind to bile acids and prevent enterohepatic circulation Decrease LDL Increase HDL	Hypercholesterolemia
Inhibitors of cholesterol absorption Ezetimibe Ezetimibe w/simvastatin	Decrease cholesterol transport into enterocytes Decrease LDL Decrease TG Increase HDL	Hypercholesterolemia
Fibrates Fenofibrate Gemfibrozil	Agonists of peroxisome proliferator-activated receptor α (PPARα) in hepatocytes Decrease TG Decrease LDL Increase HDL	Hypertriglyceridemia
Niacin Niacin Niacin w/simvastatin	Reduces free fatty acid release from adipose tissue Decreases TG Decreases LDL Increases HDL	Hypertriglyceridemia Hypercholesterolemia
Omega-3 fatty acids Omega-3-acid ethyl ester	Regulate hepatic nuclear transcription factors to reduce TG synthesis and increase fatty acid oxidation Reduces TG	Hypertriglyceridemia

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