Lipid-Lowering Drugs: What Are Your Options?

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Andrew Soundarajan

Making changes to establish a healthier lifestyle - through diet, exercise, or other healthy changes - is important to keeping your cholesterol and triglyceride levels healthy. Sometimes, however, this may not work, and your healthcare provider may want to place you on medication.

Many cholesterol-lowering medications are currently on the market, and each of these medications lower cholesterol and/or triglyceride levels in different ways.

Additionally, each of these drugs target different aspects of your lipid profile. For instance, some drugs may only be effective in lowering your LDL cholesterol levels, whereas other drugs may target every aspect of your lipid profile. In any case, your healthcare provider will weigh the benefits and risks of each drug, and select the best lipid-lowering drugs that are right for you. These prescription medications are currently on the market:

Statins

Statins, also known as HMG-CoA reductase inhibitors, are the most commonly prescribed cholesterol-lowering medications. Although they have received a bad reputation for some of the undesirable, but rare, side effects, they target every aspect of your lipid profile.

Statins can decrease LDL between 18 and 65%, increase HDL (the “good” cholesterol) up to 5 to 15% percent, and decrease triglycerides by 7 to 30%. Not only are statins effective in normalizing all aspects of your cholesterol profile, they have been also noted to prevent death and complications due to cardiovascular disease.

Statins also possess anti-inflammatory properties that help slow the progression of atherosclerosis that can lead to cardiovascular disease. With these extra benefits of statins, these drugs are the most widely prescribed of the cholesterol-lowering medications. The following drugs are classified as statins:

  • Rosuvastatin (Crestor)
  • Atorvastatin (Lipitor)
  • Simvastatin (Zocor)
  • Lovastatin (Mevacor)
  • Pravastatin (Pravachol)
  • Fluvastatin (Lescol)

Bile Acid Resins

Bile acid resins reduce cholesterol in the blood by preventing bile acids from being reabsorbed. They typically work on LDL cholesterol, reducing it by between 15 to 30% and slightly increasing HDL by 3 to 5%. Typically, triglycerides are not touched by bile acid resins – and may actually raise triglycerides levels. Additionally, some vitamins and drugs cannot be taken around the time you take bile acid resins, since their absorption is limited and may make them ineffective. The following medications are classified as bile acid resins:

  • Cholestyramine (Questran)
  • Colestipol (Colestid)
  • Colesevelam (Welchol)

Fibric Acids

Fibric acids, or fibrates, are most noted for their ability to lower triglycerides, which can be lowered on an average of 20 to 50%. They also lower LDL levels by between 5 to 20% and can raise HDL levels by 10 to 20%. This class of drugs has been known to produce muscle toxicity, especially when combined with other drugs such as statins and warfarin (Coumadin®).

In this case, your healthcare provider may either adjust the dose of your drug (as in the case of warfarin). The following medications are fibrates:

  • Gemfibrozil (Lopid)
  • Fenofibrate (Tricor)

Absorption Inhibitors

Ezetimibe is currently the only drug in this class and primarily targets LDL cholesterol levels, lowering LDL levels by an average of 15 percent. Typically, ezetimibe is coupled with a statin to ensure a powerful effect when lowering LDL levels.  Although these medications have been shown to lower LDL, they have not been shown to directly prevent the development of cardiovascular disease when used alone. Ezetimibe (Zetia) is the only FDA-approved medication within this drug class.

Omega-3 Fatty Acids

Although there are over-the-counter omega-3 fatty acids available, prescription omega-3 fatty acid products have undergone more extensive testing to evaluate their effectiveness and safety. These products contain docosahexaenoic acid (DHA) and eicosohexaenoic acid (EPA) like the supplements found in stores, but these components are more purified and concentrated in comparison to over-the-counter supplements. Prescription omega-3 fatty acids are primarily used in individuals to target very high triglyceride levels, lowering triglycerides by up to 45%. There are currently three prescription omega-3 fatty acid [products available:

  • Epanova (omega-3 carboxylic acids)
  • Lovaza (omega-3 free fatty acids)
  • Vascepa (icosapent)

Orphan Drugs

Some lipid-lowering medications are only prescribed to individuals with very high LDL cholesterol levels. These medications are typically prescribed in cases where someone has an inherited condition that causes very high lipid levels at a young age, and other medications – such as statins – are not helping lower LDL levels. Some of these medications can cause serious side effects, such as liver disease, so they are usually dispensed under a special program by healthcare professionals who are familiar with the medication. These medications are also newer on the market and work in unique ways to lower lipid levels:

  • Antisense inhibitors: Medications in this drug class complementary bind to the section of messenger RNA that codes for making apo B-100, reducing the amount of apo B-100 made in the body. This lowers the amount of VLDL and LDL cholesterol. These drugs include Kynamro (mipomersen), which lowers LDL by about 25%.
  • PCSK9 inhibitors:  These drugs block the PCSK9 protein from interacting with LDL receptors and causing them to be degraded. This will allow LDL receptors to continue to function by removing LDL from the body – resulting in lowered LDL cholesterol levels by about 50% in studies. Drugs in this class include Repatha (evolocumab) and Praluent (alirocumab).
  • MTTP inhibitors: These drugs lower LDL cholesterol by blocking microsomal triglyceride transfer protein (MTTP), a molecule in the body that prevents VLDL and chylomicrons from being made in the liver. Juxtapid (lomitapide) is the only approved medication in this class of drugs and lowers LDL by about 50%.

Sources:

Third Report of the National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults (PDF), July 2004, The National Institutes of Health: The National Heart, Lung, and Blood Institute.

Dipiro JT, Talbert RL. Pharmacotherapy: A Pathophysiological Approach, 9th ed 2014.

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