Highlights
- Hypercholesterolemia, also known as high cholesterol, can increase your risk for heart attack or stroke.
- The most commonly used cholesterol drugs work to lower low density lipoprotein (LDL) cholesterol, often referred to as bad cholesterol. Some drugs work to lower triglycerides (blood fats) and also help to increase high-density lipoprotein (HDL) in the bloodstream.
- The right cholesterol medication for you will depend on your current health status, lifestyle, and personal health factors.
- BidRx can help you get the best prices for cholesterol medications.
Finding the right combination of cholesterol medication and lifestyle changes can get you on track for better lifelong health. The right medication for you will depend on your existing health status, other medications you may be taking, and risk for certain side effects.
About Cholesterol-lowering Medications
Cholesterol medications are prescribed to treat hypercholesterolemia, more commonly referred to as high cholesterol or elevated cholesterol. This common condition can contribute to a number of chronic health conditions, including heart attack and stroke. Fortunately, there are safe and effective medications available to treat high cholesterol.
The effectiveness of cholesterol medications will vary from person to person. Medications are most effective when combined with a healthy diet and exercise regimen. The best medication for you will depend on your personal health and lifestyle factors.
Major classes of cholesterol medications include:
- Statins
- Cholesterol absorption inhibitor
- PCSK9 inhibitors
- ACL inhibitors
- Bile acid sequestrants
- Fibrates
- Niacin
- Omega-3 fatty acids
Statins

Statins are a class of drugs that work in the liver to prevent cholesterol from forming. This helps to reduce the total amount of cholesterol circulating through your bloodstream. Statins are the most commonly prescribed class of cholesterol medications.
Statins are effective at treating LDL (bad) cholesterol. They can also help lower triglycerides and raise HDL (good) cholesterol.
Examples of statins include:
- Atorvastatin (Lipitor)
- Fluvastatin (Lescol XL)
- Lovastatin (Altoprev)
- Pitavastatin (Livalo)
- Pravastatin (Pravachol)
- Rosuvastatin (Crestor)
- Simvastatin (Zocor)
Some people benefit from taking combination medications that contain statins.
Common combination statin medications include —
- Atorvastatin + amlodipine (Caduet)
- Simvastatin + ezetimibe (Vytorin)
Warnings and Contraindications — Statins
People with certain health conditions may experience additional risks or side effects when taking statins. Statins are not safe for women who are pregnant or planning to become pregnant. You should also never take statins if you have active or chronic liver disease.
Side Effects — Statins
Talk to your provider about potential side effects before taking statins. Most side effects are considered mild and resolve after your body adjusts to taking statins. However, your provider may wish to perform routine liver function tests to monitor for serious side effects.
Potential side effects of statins include:
- Constipation
- Cramps
- Diarrhea
- Elevation of liver enzymes
- Increased blood sugar levels
- Muscle pain
- Stomach pain
Drug Interactions — Statins
Statins commonly interact with other heart drugs. Speak to your provider about potential drug interactions before taking statins.
Cholesterol Absorption Inhibitors
Cholesterol absorption inhibitors treat hyperlipidemia by lowering LDL cholesterol and total cholesterol. This class of drug is the most common kind of non-statin agent used to treat high cholesterol.
Cholesterol absorption inhibitors work in the intestines to reduce the absorption of dietary and biliary cholesterol. This helps to reduce the amount of intestinal cholesterol delivered to the liver. This results in increased LDL receptor activity, which leads to increased clearance of LDL cholesterol from the bloodstream.
Ezetimibe (Zetia) is the first cholesterol absorption inhibitor.
Warnings and Contraindications — Zetia
People with certain health conditions may experience additional risks or side effects when taking cholesterol absorption inhibitors. These drugs may not be safe for women who are pregnant or planning to become pregnant. You should also avoid taking cholesterol absorption inhibitors while breastfeeding.
Side Effects — Zetia
Talk to your provider about potential side effects before taking cholesterol absorption inhibitors.
Potential side effects include:
- Diarrhea
- Fatigue
- Muscle soreness
- Stomach pain
Drug Interactions — Zetia
There are currently no documented major drug interactions for Zetia. Talk to your provider about potential drug interactions prior to using this cholesterol drug.
PCSK9 Inhibitors
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is an enzyme that binds to LDL receptors. By binding to LDL receptors, LDL can’t be cleared from the bloodstream, and cholesterol rises. PCSK9 inhibitors block these enzymes, which frees up LDL receptors to clear LDL from the bloodstream.
These are powerful LDL-lowering drugs that may be used if statins have been ineffective at lowering your cholesterol. These drugs are administered via injection.
Examples of PCSK9 inhibitors include:
- Alirocumab (Praluent)
- Evolocumab (Repatha)
Warnings and Contraindications — PCSK9 Inhibitors
Talk to your provider about your current health status and any concerns you have prior to taking PCSK9 inhibitors.
Side Effects — PCSK9 Inhibitors
Long term side effects of PCSK9 inhibitors have not yet been established in clinical research.
Potential short term side effects include:
- Itching
- Pain or bruising at the injection site
- Swelling
Drug Interactions — PCSK9 Inhibitors
You can safely take PCSK9 inhibitors with other drugs, under the direction of your medical provider.
ACL Inhibitors
Adenosine triphosphate-citrate lyase (ACL) inhibitors block the production of cholesterol in the liver. They are commonly combined with statins to reduce LDL cholesterol in adults with familial heterozygous hypercholesterolemia and in patients with heart disease.
Examples of ACL inhibitors include:
- Bempedoic acid (Nexletol)
- Bempedoic acid-ezetimibe (Nexlizet)
Warnings and Contraindications — ACL Inhibitors
Talk to your provider about your current health status and any concerns you have prior to taking ACL inhibitors.
Side Effects – ACL Inhibitors
Talk to your provider about potential side effects before taking ACL inhibitors.
Potential side effects of ACL inhibitors include:
- Acute gout
- Increased risk of tendon rupture or injury
- Joint pain
- Muscle spasms
Drug Interactions — ACL Inhibitors
There are currently no documented major drug interactions for ACL inhibitors. Talk to your provider about potential drug interactions prior to using this cholesterol drug.
Bile Acid Sequestrants
Bile acid sequestrants are also called bile acid-binding agents. These drugs work by helping the intestine get rid of cholesterol. They can reduce LDL cholesterol and help to increase HDL cholesterol in the bloodstream.
Due to common gastrointestinal (GI) side effects, these drugs are not as frequently prescribed as they were in the past.
Examples of bile acid sequestrants include:
- Cholestyramine (Prevalite)
- Colesevelam (Welchol)
- Colestipol (Colestid)
Warnings and Contraindications — Bile Acid Sequestrants
People with certain health conditions may experience additional risks or side effects when taking bile acid sequestrants. For example, these drugs may not be safe for people with intestinal blockages, bile disorders, or other GI conditions.
Side Effects — Bile Acid Sequestrants
The most common side effects of bile acid sequestrants are GI issues.
Potential side effects of bile acid sequestrants include:
- Bloating
- Constipation
- Cramping
- Gas
- Heartburn
- Nausea
- Upset stomach
Drug Interactions — Bile Acid Sequestrants
Bile acid sequestrants may decrease the absorption of other drugs. This includes thyroid hormones, diuretics, and many other drugs. Talk to your provider about potential drug interactions prior to using this cholesterol drug.
Fibrates
Fibrates are a popular drug used to lower triglyceride levels. They are effective at lowering triglycerides, but can also help to lower LDL and to raise HDL in the bloodstream.
Fibrates are believed to work by activating a protein known as PPAR-alpha. The PPAR-alpha protein in turn activates the enzyme lipoprotein lipase, which helps to reduce triglycerides and overall LDL cholesterol.
Examples of fibrates include:
- Fenofibrate (Antara, Lipofen)
- Gemfibrozil (Lopid)
Warnings and Contraindications — Fibrates
People with certain health conditions may experience additional risks or side effects when taking fibrates. For example, people with active or chronic liver disease, gallbladder disease, or renal dysfunction should avoid taking fibrates.
Side Effects — Fibrates
Potential side effects of fibrates include:
- Muscle pain
- Nausea
- Stomach pain
Drug Interactions — Fibrates
Fibrates should not be taken with statins. Talk to your provider about potential drug interactions prior to using this cholesterol drug.
Niacin
Niacin is a B vitamin that helps to control the production of triglycerides in the liver. By reducing the production of triglycerides, niacin can also help to reduce LDL cholesterol.
Niacin is available by prescription. Examples include:
Warnings and Contraindications — Niacin
People with certain health conditions may experience additional risks or side effects when taking niacin. People with active or chronic liver disease or who have a history of stomach ulcers should not take niacin. People with diabetes should also use caution when using niacin, as it may increase blood sugar levels.
Side Effects — Niacin
Most side effects from niacin are temporary. However, your provider may wish to monitor your liver functions while taking niacin, as it can cause toxicity.
Potential side effects of niacin include:
- Abnormal liver function
- Facial and neck flushing (warmth, redness, or tingling)
- Headache
- Increased blood sugar
- Itching
- Upset stomach
Drug Interactions — Niacin
Niacin may reduce the effectiveness of other medications. Avoid taking colestipol (Colestid) or cholestyramine (Locholest, Prevalite, Questran) while taking Niacin. You should only take niacin as prescribed.
Omega-3 Fatty Acids
Omega-3 fatty acids are derived from fish oils. They can be used in combination with dietary changes to help people reduce their triglyceride levels. They are typically taken in large doses when used to treat high cholesterol and should only be taken for this purpose under the direction of your provider.
It is believed that omega-3 fatty acids work to lower cholesterol by reducing very low density lipoprotein (VLDL) production in the liver. This helps to lower triglycerides and may also help to increase HDL cholesterol in the bloodstream.
Omega-3 fatty acids are available by prescription. Examples include:
Warnings and Contraindications — Omega-3 Fatty Acids
People with certain health conditions may experience additional risks or side effects when taking omega-3 fatty acids. You should not take omega-3 fatty acids if you are allergic to them or have a soybean allergy. Omega-3 fatty acids may not be safe to take for women who are pregnant or breastfeeding.
Speak to your provider about the safety of taking omega-3 fatty acids if you have:
- A shellfish allergy
- Diabetes
- Liver disease
- A heart rhythm disorder
- A thyroid disorder
- A pancreas disorder
Side Effects — Omega-3 Fatty Acids
Side effects from omega-3 fatty acids are typically mild and temporary.
Potential side effects of omega-3 fatty acids include:
- Belching
- Having a fishy taste in your mouth
- Indigestion
- Increased risk of bleeding
- Loss of appetite
Drug Interactions — Omega-3 Fatty Acids
Talk to your provider about potential drug interactions prior to using this cholesterol drug.
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