What types of drugs are used to lower cholesterol?

Cholesterol is produced in the body by the liver, but is also taken in from food derived from animals (such as meat and dairy products.) You might have a genetic issue that leads to high blood cholesterol levels, or your cholesterol might be high due to food choices and lack of physical activity. You can improve cholesterol levels with a healthy diet and exercise, but if the cholesterol level doesn’t drop low enough to be healthy, your healthcare provider might prescribe medication.

There are several classes of drugs used to decrease cholesterol. These include:

  • Statins.
  • PCSK9 inhibitors.
  • Fibric acid derivatives (also called fibrates).
  • Bile acid sequestrants (also called bile acid resins).
  • Nicotinic acid (also called niacin).
  • Selective cholesterol absorption inhibitors.
  • Omega 3 fatty acids and fatty acid esters.
  • Adenosine triphosphate-citrate lyase (ACL) inhibitors.

Your healthcare provider will discuss these options with you and together you can decide which type of medication, if any, would be best for you.

Statins

Statins are one of the better known types of cholesterol-lowering drugs. Statins decrease cholesterol output by blocking the HMG CoA reductase enzyme that the liver uses to make cholesterol. Statins are also called HMG CoA reductase inhibitors.

Statins also:

  • Improve the function of the lining of the blood vessels.
  • Reduce inflammation (swelling) and damage.
  • Reduce the risk of blood clots by stopping platelets from sticking together.
  • Make plaques (fatty deposits) less likely to break away and cause damage.

These additional benefits help prevent coronary vascular disease (CVD) in people who have had events like heart attacks and in people who are at risk.

What statins are available to treat high cholesterol?

Available statin drugs

Generic name (brand name)

Common dosage

in milligrams (mg)

Atorvastatin (Lipitor®)10 to 80 mg daily
Fluvastatin (Lescol®, Lescol XL®)20 to 80 mg daily (or split twice daily)
Lovastatin (Mevacor®, Altoprev®)20 to 80 mg daily
Pitavastatin (Livalo®, Zypitamag™)2 to 4 mg daily
Pravastatin (Pravachol®)10 to 80 mg daily
Rosuvastatin (Crestor®)5 to 40 mg daily
Simvastatin (Zocor®)5 to 40 mg daily

What are the side effects of statins?

Like any other drugs, statins may produce unwanted side effects. These may include:

  • Constipation or nausea.
  • Headaches and cold-like symptoms.
  • Sore muscles, with or without muscle injury.
  • Liver defects.
  • Increased blood glucose levels.
  • Reversible memory issues.

If you’re unable to take statins because of the side effects, you’re said to be statin-intolerant. If you are taking a statin, you should avoid grapefruit products because they can increase side effects. You should limit the amount of alcohol that you drink because combining alcohol and statin usage can increase your risk of liver damage. You may want to talk with your provider or pharmacist if you are concerned about any other types of interactions.

PCSK9 inhibitors

PCSK9 inhibitors are designed to attach to a particular liver protein, which results in lowered LDL cholesterol. This class of drug can be given with statins and is usually for people at high risk of heart disease who have not been able to lower their cholesterol enough through other means.

What PCSK9 inhibitors are available to treat cholesterol?

Available PCK9 inhibitors Generic name (brand name)Common dosages
in milligrams (mg)
Alirocumab (Praluent®)Initially 75 mg once every two
weeks or 300 mg every four weeks; if response is inadequate, dose may increase to a maximum of 150 mg every two weeks by injection.
Evolocumab (Repatha®)140 mg every two weeks
or 420 mg once a month by injection.

What are some possible side effects of PCSK9 inhibitors?

Possible side effects include pain, including muscle pain (myalgia) and back pain, or swelling at the injection site and cold-like symptoms. Another drawback may be cost as these products may be expensive.

Fibric acid derivatives (fibrates)

Fibric acid derivatives make up another class of drugs that reduce blood lipid (fat) levels, especially triglycerides. Triglycerides are fats that come from food that are created when you consume calories that are not spent.

Fibric acid derivatives may also increase the level of HDL, also called the “good” cholesterol, while lowering liver production of LDL, the “bad” cholesterol. People who have severe kidney disease or liver disease should not take fibrates.

What fibrates are available to treat high cholesterol levels?

Fibric acid derivatives

Generic name (brand name)

Common dosages

in milligrams (mg)

Fenofibrate (Tricor®, Antara®, Fenoglide®, Fibricor®,Lipidil®, Lipofen®, Triglide®, Trilipix®)Dose varies.

Gemfibrozil (Lopid®)*

*Gemfibrozil should not be taken with statins.

600 mg twice daily. Take 30 minutes before you eat breakfast and dinner.

What are some possible side effects of fibric acid derivatives?

Possible side effects of fibrates include:

  • Constipation or diarrhea.
  • Weight loss.
  • Bloating, belching or vomiting.
  • Stomachache, headache or backache.
  • Muscle pain and weakness.

Bile acid sequestrants (also called bile acid resins)

This class of drugs works inside the intestine by attaching themselves to bile, a greenish fluid made of cholesterol that is produced by the liver to digest food. The binding process means that less cholesterol is available in the body. Resins decrease LDL cholesterol and give a slight boost to HDL cholesterol levels.

What bile acid resins are available to treat cholesterol?

Available bile acid resins

Generic name (Brand name)

Dosages
Cholestyramine (Questran®)4 – 16 g/day (once or twice daily). The dose of 4 grams one to two times per day should be increased gradually over about one month intervals to 8-16 g/day divided into two doses. The maximum dose is 24 g/day taken in divided doses.
Colestipol (Colestid®)Granule formulation: 5 g once or twice a day increase by 5 g every 1 to 2 months if needed. Maintenance dose: 5 to 30 g/day once daily or in divided doses.
Tablet formulation: 2 g once or twice a day increase by 2 g once or twice daily every 1 to 2 months if needed. Maintenance dose: 2 to 16 g/day once daily or in divided doses.
Colesevelam (Welchol®)3.75 g/day in one to two divided doses. Product comes in tablet or powder form.

What are the possible side effects of bile acid resins?

Possible side effects of bile acid sequestrants include:

  • Sore throat, stuffy nose.
  • Constipation, diarrhea.
  • Weight loss.
  • Belching, bloating.
  • Nausea, vomiting, stomach pain.

If your medication is a powder, never take it dry. It must always be mixed with at least three to four ounces of liquid such as water, juice or a noncarbonated beverage.

If you take other medications besides these, make sure you take the other drugs one hour before or four hours after taking the bile acid resin.

Selective cholesterol absorption inhibitors

This class of medication works in the intestine to stop the body from absorbing cholesterol. These inhibitors reduce LDL cholesterol, but may also help with triglycerides and HDL cholesterol. They can be combined with statins.

There is one product of this class currently available: ezetimibe (Zetia®). The usual dose is 10 mg/day. Possible side effects include diarrhea, fatigue and joint pain.

Nicotinic acid

Nicotinic acid, also called niacin, is a B-complex vitamin. You can get over-the-counter versions of this, but some versions are prescription only. Niacin decreases LDL cholesterol and triglycerides and increases HDL. If you have gout or severe liver disease, you should not take niacin.

What nicotinic acid products are available to treat cholesterol levels?

Available nicotinic acid products

Generic name (Brand name)

Dosages
Extended release niacin (Niaspan®)1-2 g/day once daily at bedtime.
Immediate release niacin (Niacor®)1.5-3 g/day (divide daily dose up to to three times per day).
Sustained release (Slo-Niacin®) or over-the-counter niacin products.Take 250-750 mg once per day, morning or evening or as directed. Consult your
provider before using
more than 500 mg /d.

What are possible side effects of niacin?

The main side effect of niacin is flushing of the face and upper body, which might be lessened if you take it with meals. You might have less flushing if you take aspirin about 30 minutes before taking niacin.

Other side effects include:

  • Skin issues, such as itching or tingling.
  • Headache.
  • Stomach upset.
  • Can lead to increased blood sugars.
  • Coughing.
Omega-3 fatty acid esters and polyunsaturated fatty acids (PUFAs)

These kinds of drugs, used to lower triglycerides, are commonly called fish oils. Some products are available as OTC items, while others are prescription only. Here are two things to consider: Fish oils might interfere with other medications, and some people are allergic to fish and shellfish.

What omega-3 products are available to treat cholesterol levels?

Available omega-3 products

Generic name (Brand name)

Dosages
Icosapent ethyl (Vascepa®) 2 g twice daily with meals.
Omega-3-acid ethyl esters (Lovaza®)2 g twice daily.

What are the possible side effects of omega 3 products?

Possible side effects of omega-3 products include:

  • Belching.
  • Skin issues like rash or itching.
  • Gas.
  • Fishy taste.
  • Increased bleeding time.

Adenosine triphosphate-citric lyase (ACL) inhibitors

The FDA has approved bempedoic acid (Nexletol™) to lower cholesterol. Bempedoic acid works in the liver to slow down cholesterol production. The medication comes in 180-mg tablets taken once per day with or without food. It should be taken with statin medications, but there are dosage limitations if taken with simvastatin or pravastatin.

What are the possible side effects of bempedoic acid?

Some possible side effects of bempedoic acid include:

  • Upper respiratory infection.
  • Stomach, back or muscle pain.
  • Increased levels of uric acid.
  • Tendon injury.

What about using red rice yeast or plant stanols (phytosterols) instead of prescription drugs to lower cholesterol?

Many people say they prefer to take ‘natural’ medicines over prescription drugs. However, just because something is natural doesn’t mean that it’s safe. In the U.S., supplements are not regulated as closely as medicines. Supplements can also interfere in dangerous ways with medications that you already take.

However, red rice yeast extract does contain lovastatin, which is the same chemical that is in Mevacor. In some cases, you and your healthcare provider might agree that you should try the supplement with monitoring.

Plant stanols are another nonprescription choice for lowering cholesterol. Plant stanols work by stopping the body from absorbing cholesterol in the intestines. One brand is CholestOff® capsules, while plant stanols are also available in margarine substitutes like Benecol®.

How to take your cholesterol-lowering medicines

When you are taking medicines, it is important to follow your healthcare provider’s advice carefully. If you don’t take medicines exactly as prescribed, they can harm you. For example, you could unknowingly counteract one medicine by taking it with another one. Medicines can make you feel sick or dizzy if not taken properly.

Taking your medicine

Medicine can only help you reduce cholesterol if you take it correctly. You should take all medicines as advised by your provider. Don’t hesitate to let them know if you don’t think the medication is working or if you have side effects that concern you. Fill your prescriptions regularly, and don’t wait till you are out of something to get a refill.

You can ask your healthcare provider or pharmacist any questions you have. Let them know if you have problems getting to the pharmacy to pick up your medicines or if the instructions are too complicated. If you have trouble understanding your provider or pharmacist, ask a friend or family member to be with you when you ask questions. You need to know what medicines you take and what they are for.

Don’t decrease your medicine dosage to save money. You must take the full amount to get the full benefits. If your medicines are too expensive, ask your provider or pharmacist about finding financial assistance. Some companies provide discounts for certain medications.

There are now many ways to keep track of medication schedules. It might help to have a routine of taking your medicines at the same time every day. You can have a pillbox marked with the days of the week that you fill at the start of the week. Some people keep a medication calendar or journal, marking down the time and date and dose. Make use of smart phone apps and pillboxes with alarms you can set.

If you forget to take a dose, take it as soon as you remember. However, if it’s almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Don’t take two doses to make up for the dose you missed.

When traveling, keep your medicines with you so you can take them as scheduled. On longer trips, take an extra week's supply of medicines and copies of your prescriptions, in case you need to get a refill.

Always discuss any new medication with your provider, including over-the-counter drugs, herbal or dietary supplements. Your cholesterol medicine dose might have to be adjusted. Make sure you tell your dentist and other providers what medications you are taking, especially before having surgery with a general anesthetic.

All of your medicines to lower cholesterol will be more effective if you continue to follow a low cholesterol diet. Your healthcare provider may be able to refer you to a dietitian for help in designing a diet especially for you and encouraging you to stay with it.

A note from Cleveland Clinic

You may need medications to improve your cholesterol numbers. There are several options, but any of them will work better if you eat healthy and exercise. Remember to discuss any new medication with your provider. This includes over-the-counter products like herbs or dietary supplements.

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