Medications and Supplements To Help Lower Cholesterol
Explore the major classes of cholesterol-lowering drugs, their effectiveness, side effects, and who should consider using them.
Managing cholesterol is essential for reducing the risk of heart disease and stroke. For many, lifestyle changes such as diet and exercise may not be enough, making medications and specific supplements vital in treating high cholesterol. This article provides a comprehensive guide to the major types of cholesterol-lowering drugs and supplements, their effectiveness, risks, and practical considerations for use.
Understanding Cholesterol and Cardiovascular Risk
Cholesterol is a waxy substance present in every cell of your body, necessary for building healthy cells. However, high levels of low-density lipoprotein (LDL), often called “bad cholesterol,” can increase your risk of heart disease and stroke. High-density lipoprotein (HDL) or “good cholesterol” helps remove unwanted cholesterol from your bloodstream.
Excess cholesterol can build up in your blood vessels, forming plaques that may narrow or block arteries, leading to heart attacks or strokes. Medications can help manage these risks when lifestyle modification is insufficient.
Statins
Statins are the most commonly prescribed class of drugs for lowering cholesterol. They work by decreasing cholesterol production in the liver, helping the body remove excess cholesterol from the blood.
Statins have been shown to:
- Lower LDL (bad) cholesterol levels significantly.
- Reduce the risk of heart attack and stroke.
- Lower triglycerides (blood fats).
- Modestly raise HDL (good) cholesterol.
Examples of statins include:
- Atorvastatin (Lipitor)
- Fluvastatin (Lescol)
- Lovastatin (Altoprev, Mevacor)
- Pitavastatin (Livalo)
- Pravastatin (Pravachol)
- Rosuvastatin (Crestor)
- Simvastatin (Zocor)
Statins may also be combined with other cholesterol-lowering medications for increased effectiveness, such as:
- Simvastatin with ezetimibe (Vytorin)
- Atorvastatin with amlodipine (Caduet)
How Statins Work
Statins block the enzyme HMG-CoA reductase in the liver, decreasing the production of cholesterol. This lower cholesterol production stimulates the liver to remove more LDL cholesterol from the bloodstream.
Effectiveness
Statins can lower LDL cholesterol by up to 60% and are the mainstay of therapy for most individuals with high cholesterol, high cardiovascular risk, or existing heart disease.
Potential Side Effects
- Muscle pain or weakness
- Dizziness or headache
- Constipation, diarrhea, or upset stomach
- Nausea and gas
- Rarely, muscle damage or breakdown
- Very rarely, liver damage or new-onset type 2 diabetes
Risks and Contraindications
- If you have liver disease, you may need a lower dose or different medication.
- Statins should not be taken during pregnancy or breastfeeding.
- Some statins interact with certain foods, especially grapefruit, and with particular medications.
PCSK9 Inhibitors
What others are reading
PCSK9 inhibitors are a newer class of cholesterol-lowering drugs. These are monoclonal antibodies that target the PCSK9 protein, which can affect how the liver handles cholesterol. By inactivating this protein, your liver removes more cholesterol from the blood.
| Drug Name | Brand Name | Dosage Form |
|---|---|---|
| Alirocumab | Praluent | Injection every 2–4 weeks |
| Evolocumab | Repatha | Injection every 2–4 weeks |
PCSK9 inhibitors are particularly valuable for people with genetic forms of high cholesterol (familial hypercholesterolemia) or for those who cannot reach their cholesterol goals with statins alone.
Effectiveness
- Significantly lower LDL cholesterol when added to statin therapy.
- Shown in large studies to reduce cardiovascular events such as heart attacks and strokes.
Potential Side Effects
- Bruising, pain, or swelling at the injection site
- Cold-like symptoms
- Rare reports of cognitive problems, though a clear connection has yet to be proven
Risks and Considerations
- Allergic reactions are rare but possible.
- People with latex allergies should use caution with evolocumab formulations that may contain latex.
- PCSK9 inhibitors can be expensive, so insurance coverage may be required for access.
Adenosine Triphosphate-Citrate Lyase (ACL) Inhibitors
ACL inhibitors work by blocking a liver enzyme needed to produce cholesterol, leading to increased LDL removal from the bloodstream. Approved in 2020, bempedoic acid is currently the main drug in this class and may be used alone or with ezetimibe as a combination pill.
- Bempedoic acid (Nexletol)
- Bempedoic acid + ezetimibe (Nexlizet)
How They Work
These drugs are usually taken orally and often used for people who can’t tolerate statins or who need additional cholesterol lowering beyond what statins provide. ACL inhibitors have shown benefits in lowering LDL cholesterol and improving outcomes when added to other therapies.
Potential Side Effects
- Increased uric acid levels, potentially increasing the risk of gout
- Possible decreased kidney function
- Abnormal blood test results in rare cases (lower platelets, leukocytes, or hemoglobin)
Risks and Considerations
- Risk of tendon rupture, especially in people with a history of similar injuries
- Regular blood monitoring may be required
Ezetimibe
Ezetimibe decreases cholesterol absorption from the intestine, reducing the amount of cholesterol delivered to the liver.
- Often used in combination with statins or as an alternative for people who are statin-intolerant
- Lowers LDL cholesterol by around 20%
- Minimal side effects
Bile Acid Sequestrants
Bile acid sequestrants bind bile acids (which contain cholesterol) in the intestine, reducing their reabsorption and forcing the liver to use more cholesterol to produce additional bile acids. This process helps to lower LDL cholesterol by 10–30%.
Examples include:
- Cholestyramine
- Colestipol
- Colesevelam
These medications are sometimes combined with other therapies but may cause gastrointestinal side effects like constipation, gas, and bloating.
Niacin
Niacin (nicotinic acid) is a B vitamin that can lower LDL and triglycerides while raising HDL cholesterol, though its use as a primary cholesterol-lowering drug has declined due to the risk of side effects and a lack of additional benefit when used with statins.
- Potential side effects: skin flushing, itching, liver toxicity, increased blood sugar, and gout
Fibrates
Fibrates primarily lower triglyceride levels and may improve HDL cholesterol. They have a modest effect on lowering LDL cholesterol and are occasionally prescribed for people with high triglycerides.
- Gemfibrozil (Lopid)
- Fenofibrate (Tricor, Lofibra, Lipofen, others)
Possible side effects: stomach upset, muscle pain, and increased risk of gallstones. Fibrate use with statins increases the risk of muscle damage.
Omega-3 Fatty Acid Supplements
Omega-3 fatty acids, found in fish oil and certain prescription products, primarily lower triglycerides. These supplements may modestly raise HDL but typically do not lower LDL cholesterol.
Prescription omega-3 products include:
- Icosapent ethyl (Vascepa)
- Omega-3-acid ethyl esters (Lovaza)
Non-prescription omega-3 supplements are widely available, but high doses may interfere with blood clotting and should be used under medical supervision.
Other Newer and Supplementary Agents
Inclisiran
Inclisiran is a small interfering RNA (siRNA) therapy that lowers cholesterol by reducing the production of the PCSK9 protein, similar to PCSK9 inhibitors but requiring dosing only twice a year. Inclisiran is primarily reserved for certain high-risk patients.
Red Yeast Rice
This dietary supplement contains naturally occurring statin-like compounds that can lower cholesterol, but the amount of active ingredient varies and some preparations may contain contaminants. It is not typically recommended over prescription statins due to lack of regulation.
Practical Tips: Lifestyle and Medication
Drug therapy works best when combined with heart-healthy lifestyle changes:
- Adopt a diet low in saturated fat and high in fruits, vegetables, and whole grains
- Stay physically active most days of the week
- Manage your weight
- Avoid tobacco products
- Limit alcohol intake
Choosing a Drug Treatment: Individualized Approach
Not every person with high cholesterol needs medication. The decision is guided by your:
- Level of LDL cholesterol and other lipids
- Total cardiovascular risk (other health problems, age, family history)
- Response to previous therapies and tolerance of side effects
Your healthcare provider may use a risk calculator to estimate your 10-year or lifetime risk of heart attack and stroke.
Frequently Asked Questions (FAQs)
Q: When should medication for cholesterol be considered?
A: Medication is recommended when lifestyle measures are not enough to achieve target cholesterol levels, particularly in people at high risk for heart attack or stroke or those with known cardiovascular disease.
Q: How long do I need to take cholesterol-lowering medication?
A: Most people need to take these medications long-term, often for life, as cholesterol levels can rise again if medication is stopped without lifestyle changes.
Q: Can supplements replace prescription medications?
A: No, supplements may have a mild effect on cholesterol but are not a substitute for proven medications, especially in high-risk individuals.
Q: Are cholesterol-lowering drugs safe?
A: These medications are generally safe and effective. Side effects vary by drug but are usually mild. Rare, serious side effects should be discussed with your healthcare provider before starting therapy.
Q: Can I stop taking cholesterol medication if my levels improve?
A: Always consult your healthcare provider before stopping any medication. Cholesterol levels often increase again if preventative steps are not maintained.
Key Points to Remember
- Cholesterol-lowering medications can greatly reduce heart disease risk when lifestyle measures are insufficient.
- Statins remain the first-line treatment, but alternatives and add-on therapies are available for those who need them.
- Choosing the right medication depends on cholesterol levels, risk factors, response to therapy, and individual tolerance.
- Regular follow-up and cholesterol checks are essential for anyone taking these medications.
Always work with your healthcare provider to find the best strategy for managing your cholesterol and reducing your risk of cardiovascular disease.
References
- https://www.ncbi.nlm.nih.gov/books/NBK395573/
- https://www.healthline.com/health/heart-disease/cholesterol-lowering-drugs
- https://www.heart.org/en/health-topics/cholesterol/prevention-and-treatment-of-high-cholesterol-hyperlipidemia/cholesterol-medications
- https://www.mayoclinic.org/diseases-conditions/high-blood-cholesterol/in-depth/statins/art-20045772
- https://www.healthline.com/health-news/new-analysis-finds-millions-of-people-on-statins-may-not-need-them
- https://www.healthline.com/health/video/lifestyle-changes-high-cholesterol
- https://www.mayoclinic.org/diseases-conditions/high-blood-cholesterol/in-depth/cholesterol-medications/art-20050958
- https://medlineplus.gov/cholesterollevelswhatyouneedtoknow.html
- https://www.medicalnewstoday.com/articles/325113
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