Control Cholesterol with Medication


Sarah Lewis, PharmD    

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More than 30% of American adults struggle with high cholesterol, which can raise the risk of developing heart disease and stroke, two leading causes of death in the United States. Fortunately, there are plenty of tools available to get cholesterol levels down. Most of the body’s cholesterol is produced by the liver, only a portion is dietary.

Healthy lifestyle habits like eating well and staying active are often the first steps in managing high cholesterol levels. But sometimes they aren’t enough to help you reach your cholesterol goals. If your levels are still too high after 6 to 12 months, your doctor will probably prescribe medications to lower your cholesterol. If you have other risk factors for cardiovascular disease your doctor will likely initiate medical therapy sooner. Either alone or in combination, medicines work to:

  • Decrease LDL or “bad” cholesterol levels

  • Decrease triglyceride levels

  • Increase HDL or “good” cholesterol levels


Statins—or HMG-CoA reductase inhibitors—are a staple of cholesterol medication treatment. They decrease the amount of cholesterol your body naturally produces. Statins mainly work to reduce LDL, but they also have modest effects on triglycerides and HDL.

Members of this class include:

  • Atorvastatin (Lipitor)

  • Fluvastatin (Lescol)

  • Lovastatin (Mevacor)

  • Pravastatin (Pravachol)

  • Rosuvastatin (Crestor)

  • Simvastatin (Zocor)

Side effects of statins are usually mild and go away with time. But it is possible to have liver and muscle problems with these drugs. Your doctor will order periodic lab tests to check. Tell your doctor if you have muscle aches or notice changes in your stool, urine or skin color. Also, ask your doctor or pharmacist whether your statin interacts with grapefruit juice or not.


When statins aren’t enough to do the job, your doctor may prescribe resins, also known as bile acid sequestrants. They help your body use extra cholesterol so it’s not circulating in your blood. Resins bind bile in the intestine so your body can’t use it for digestion. Your body responds by making more bile from cholesterol in your blood, which lowers your LDL levels.

Resins include:

  • Cholestyramine (Locholest, Prevalite and Questran)

  • Colestipol (Colestid)

  • Colesevelam (WelChol)

Doctors rarely use resins alone to treat cholesterol. They complement statins well, so doctors may combine the two types of drugs. The main side effects of resins are digestive in nature—constipation, bloating, gas and nausea.

Cholesterol Absorption Inhibitors

Currently, there is one cholesterol absorption inhibitor on the market, ezetimibe (Zetia). It stops your intestines from absorbing cholesterol in your diet. Like statins, it mainly decreases your LDL, but has a modest effect on triglycerides and HDL. In fact, doctors often combine ezetimibe with statins. There is even a combination product—atorvastatin/ezetimibe (Vytorin)—to make your life easier.

The main side effects of ezetimibe are stomach pain, diarrhea, fatigue, and joint pain.

PCSK9 Inhibitors

PCSK9 inhibitors are new injectable medicines to treat high cholesterol. They increase the amount of LDL cholesterol your body clears from your blood. PCSK9 inhibitors have FDA approval to treat a genetic form of high cholesterol and to further lower LDL in adults who have already had a heart attack or stroke. PCSK9 inhibitors may help these select patients when statins aren’t enough.

There are two members of this class:

  • Alirocumab (Praluent)

  • Evolocumab (Repatha)

The main side effects are injection site reactions, flu-like symptoms, and allergic reactions.


Fibrates, also known as fibrinic acid derivatives, stimulate processes in your body to get rid of triglycerides. In some cases, they can also help increase HDL. But they have little effect on LDL.

Fibrates include:

  • Fenofibrate (Antara, Lofibra, Tricor and Triglide)

  • Gemfibrozil (Lopid)

Fibrates have the potential to increase the risk of muscle problems in some people who also take a statin. If your doctor decides this combination is best for you, you will need close monitoring.


Niacin, also called nicotinic acid, works in the liver to decrease LDL and triglycerides and increase HDL.

Niacin can be found over the counter as a vitamin supplement, but may cause side effects such as flushing, itching, nausea, vomiting and diarrhea. Prescription forms of niacin, like Niaspan and Niacor, are formulated to reduce side effects. You shouldn’t substitute the vitamin supplement for a prescription product—the risk of side effects is much greater.

Omega-3 Fatty Acids

Omega-3 fatty acids help decrease triglycerides. Your doctor may recommend a supplement available over the counter. There are also prescription forms for people with very high triglycerides. They are purified and concentrated to provide higher amounts of omega-3s. They include:

  • Lovaza

  • Omtryg

  • Vascepa

Tell your doctor about any fish or shellfish allergies before taking an omega-3 fatty acid product.


Coping With the Side Effects of Cholesterol Drugs

You may need to try a few treatment options for high cholesterol before finding the right one.
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Medical Reviewers: William C. Lloyd III, MD, FACS Last Review Date: Dec 5, 2017

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Medical References

  1. Cholesterol-Lowering Medicines. American Academy of Family Physicians.
  2. Cholesterol Medications: Consider the Options. Mayo Foundation for Medical Education and Research.
  3. Drug Therapy for Cholesterol. American Heart Association.
  4. First-in-Class Cholesterol Drug Approved by FDA. Pharmacy Times.   
  5. How Is High Blood Cholesterol Treated? National Heart, Lung, and Blood Institute.