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How Do Cholesterol Lowering Drugs Affect Cholesterol?

Cholesterol Lowering Drugs Work In Many Different Ways


Updated June 10, 2014

Cholesterol lowering drugs are often used as a last resort when it comes to your lipid lowering therapy - often after lifestyle modifications, such as smoking cessation, low fat diet, and exercise do not work to effectively manage your cholesterol.

Typically, eating healthy and exercising regularly are the two most essential ingredients needed to keep cholesterol levels within normal range. Sometimes, however, this may not work, and your health-care provider may want to place you on medication. Many cholesterol-lowering medications are currently on the market, and each of these medications lower cholesterol 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 (“bad” cholesterol) levels, where as other drugs may target every aspect of your lipid profile. In any case, your health-care provider will weigh the benefits and risks of each drug, and select the best cholesterol-lowering medication for you.


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 cholesterol profile. They decrease LDL between 18 and 65 percent, increase HDL (the “good” cholesterol) up to 5 to 15 percent, and decrease triglycerides by 7 to 30 percent. Not only are statins effective in normalizing all aspects of your cholesterol profile, they have been also noted to possess anti-inflammatory properties that are being further investigated in areas such as heart disease and some types of cancer. They also stabilize plaques that have already formed, thus preventing them from rupturing and causing a subsequent stroke. Statins also reduce the likelihood of developing blood clots, improve vascular function, reduce cardiac arrhythmias, and may cause plaque reduction. With these extra benefits of statins, these drugs are the most widely prescribed of the cholesterol-lowering medications. Some studies have shown a reduction in the incidence of death even in patients with normal cholesterol levels.

Bile Acid Resins

Bile acid resins reduce cholesterol absorption from the small intestine to the bloodstream. They typically work on LDL and HDL cholesterols, although they are not as effective as statins. Bile acid resins reduce LDL by 15 to 30 percent and raise HDL by 3 to 5 percent. Typically, triglycerides are not touched by bile acid resins. In some cases, they may actually raise triglycerides levels. These drugs commonly cause a lot of bloating, nausea and cramping which greatly limits their use. 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.

Nicotinic Acid

Nicotinic acid, also known as vitamin B3 or niacin, also works on all aspects of your lipid profile. However, it is most notable for raising HDL levels (up to 15 to 35 percent) and lowering triglyceride levels (by between 20 and 50 percent). It also lowers LDL, but not as much as statins. Niacin lowers LDL levels on an average between 5 to 25 percent. Flushing occurs in about 50 percent of individuals who take this drug. This symptom can be intolerable and is the most common reason why this drug is discontinued. With the exception of Niaspan® (a sustained release niacin preparation only available by prescription), sustained release niacin products tend to produce liver toxicity compared to immediate-release niacin. Additionally, the “no-flush” niacin products available over the counter are not regulated by the Food and Drug Administration and may not contain the free nicotinic acid needed to lower cholesterol. So these drugs may be ineffective.

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 percent. They also lower LDL levels by between 5 to 20 percent and raise HDL levels by 10 to 20 percent. 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 physician may either adjust the dose of your drug (as in the case of warfarin) or avoid the combination altogether (in the case of statins).

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. Triglycerides are usually not effected by ezetimibe, while HDL levels are only slightly raised (by about 5 percent). Liver and muscle problems have been reported with ezetimibe; however, the incidence of this occurrence is low.


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 Heath: The National Heart, Lung, and Blood Institute.

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