Hypolipidemic agent

Classes of hypolipidemic drugs

There are several classes of hypolipidemic drugs. They may differ in both their impact on the cholesterol profile and adverse effects. For example, some may lower the "bad cholesterol" kidney functions of the patient, evaluated against the balancing of risks and benefits of the medications. In the United States, this is guided by the evidence-based guideline from the National Cholesterol Education Program (NCEP) Adult Treatment Panel III (ATPIII).

Established

• statins are particularly well-suited for lowering LDL, the cholesterol with the strongest links to cardiovascular diseases. In studies using standard doses, statins have been found to lower LDL-C by 18% to 55%, depending on the specific statin being used. There is a risk of severe muscle damage (myopathy & rhabdomyolysis) with statins.
• hypertriglyceridemia. Fibrates typically lower triglycerides by 20% to 50%. Level of the good cholesterol HDL is also increased. Fibrates may decrease LDL, though generally to a lesser degree than statins. Similar to statins, there is a risk of severe muscle damage (myopathy & rhabdomyolysis) with fibrates.
• hyperglycemia, and may also cause liver damage.
• bile acid sequestrants (resins) are particularly effective for lowering LDL-C by sequestering the cholesterol-containing bile acids released into the gut and preventing their reabsorption from the gut. It decreases LDL by 15-30% and raises HDL by 3-5%. It has little effect on triglycerides but can cause a slight increase. Bile acid sequestrants may cause gastrointestinal problems, and may also reduce the absorption of other drugs and vitamins from the gut.
• ezetimibe (Zetia) is a selective inhibitor of dietary cholesterol absorption.
• phytosterols may be found naturally in plants. Similar to ezetimibe, phytosterols reduce the absorption of cholesterol in the gut. Hence, they are most effective when consumed with meals. However, the precise mechanism of action of phytosterols differs from ezetimibe.

Investigational

Investigational classes of hypolipidemic agents:

• CETP Inhibitors (cholesteryl ester transfer protein inhibitors) are still under development. It is expected that these drugs will mainly increase HDL while lowering LDL.
• squalene synthase inhibitor
• ApoA-1 Milano
• AGI-1067

See also

• ATC code C10