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These studies suggest that cholesterol medications include statins, nonstatin lipid-modifying therapies like ezetimibe and PCSK9 inhibitors, oligonucleotide therapeutics, mipomersen, and plant stanols and sterols.
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Cholesterol-lowering medications are essential in managing hypercholesterolemia and reducing the risk of atherosclerotic cardiovascular disease (ASCVD). This article provides an overview of the various classes of cholesterol medications, their efficacy, and their usage trends.
Statins are the most widely used cholesterol-lowering medications. They work by inhibiting the enzyme HMG-CoA reductase, which plays a crucial role in cholesterol synthesis in the liver. Common statins include:
Statins have shown significant benefits in both primary and secondary prevention of cardiovascular events. Approximately 71% of adults with diagnosed cardiovascular disease (CVD), 63% of those with diabetes, and 54% of those with hypercholesterolemia reported taking prescription cholesterol-lowering medications. The use of statins has increased significantly over the years, with a notable rise in prescription rates from 2003 to 2012.
Ezetimibe works by inhibiting the absorption of cholesterol in the intestine. It has been shown to reduce ASCVD morbidity when used in combination with statins. For instance, the IMPROVE-IT trial demonstrated that ezetimibe/simvastatin reduced the primary outcome by 1.8% over seven years.
PCSK9 inhibitors, such as evolocumab and alirocumab, have shown significant benefits in reducing ASCVD events. The FOURIER study reported a 1.5% reduction in the primary outcome over 2.2 years with evolocumab, while the ODYSSEY OUTCOMES trial found a 1.6% reduction over 2.8 years with alirocumab.
There is minimal evidence supporting the use of niacin or cholesterol-ester transfer protein inhibitors in reducing ASCVD risk when added to statin therapy.
A new class of cholesterol-lowering drugs, oligonucleotide therapeutics, includes small interfering RNA (siRNA) molecules that destroy RNA before protein synthesis. These drugs represent a promising addition to cholesterol-lowering strategies.
Mipomersen, an antisense inhibitor of apolipoprotein B synthesis, has shown efficacy in lowering LDL cholesterol concentrations in patients with homozygous familial hypercholesterolemia. A study reported a significant reduction in LDL cholesterol levels with mipomersen compared to placebo.
Foods enriched with plant stanols or sterols can lower serum cholesterol levels. A meta-analysis showed that an intake of 2 grams per day of stanols or sterols reduced LDL cholesterol by 10%. These effects are additive with diet or drug interventions, making them a valuable option for individuals at increased risk for coronary heart disease.
Cholesterol-lowering medications, particularly statins, play a crucial role in managing hypercholesterolemia and reducing the risk of ASCVD. Nonstatin therapies like ezetimibe and PCSK9 inhibitors offer additional benefits, while emerging therapies such as oligonucleotide therapeutics and mipomersen provide new avenues for treatment. Plant stanols and sterols also offer a dietary approach to lowering cholesterol levels. The choice of therapy should be tailored to individual patient needs and risk profiles.
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