Cholesterol-Lowering Drugs

Cholesterol-Lowering Drugs

Cholesterol is a type of fat present in the blood. It is produced by the liver and is found in animal products, such as meat, poultry, and whole milk products. Small amounts of cholesterol are needed for the body to grow and for organs to function properly. However, too much cholesterol in the blood can clog arteries and lead to serious health problems.

There are two main types of cholesterol: high-density lipoprotein (HDL) and low-density lipoprotein (LDL). HDL cholesterol is considered the “good” type of cholesterol. It removes cholesterol from the blood, sends it back to the liver, and removes it from the body through urination. LDL, on the other hand, is considered the “bad” type of cholesterol. It attaches itself to blood vessels and blocks blood flow. This blockage causes the heart to work harder than it should. As a result, people with high LDL levels have an increased risk of heart disease, heart attack and stroke. That’s why it’s important to lower the level of LDL in your blood.

Healthy food choices and increased physical activity are usually the first steps to improving cholesterol. However, diet and lifestyle modifications may not work for some people. If this is the case, your doctor may recommend medications that lower LDL cholesterol or increase HDL cholesterol. Here is a list of medications that can be used to treat high cholesterol.


Statins reduce the production of cholesterol in the liver and help remove excess cholesterol from the blood vessels. Statins are very effective in lowering LDL cholesterol, but they only slightly improve HDL cholesterol levels. Here are some examples of statins

  • Atorvastatin
  • Fluvastatin (fluvastatin)
  • Lovastatin (Altoprev, Mevacor)
  • Pitavastatin (Rivastigmine)
  • Pravastatin (Pravachol)
  • Rosuvastatin calcium
  • Simvastatin

Do not take statins if you have liver disease or are pregnant. You should also avoid drinking grapefruit juice while taking this medication.

Side effects of statins include

  • constipation
  • diarrhea
  • dizziness
  • Gas
  • headache
  • Abdominal pain
  • Muscle pain

Statins are also included in combination with other cholesterol-lowering medications for additional benefits. These include the following

  • Lovastatin and niacin (Advicor)
  • Simvastatin and ezetimibe (Vytorin)
  • Atorvastatin and amlodipine (Caduet)

Do not take Vytorin or Advicor if you are pregnant or breastfeeding, or if you have liver disease. As with statins, you should not drink grapefruit juice while taking these combined medications. Side effects may include the following

  • headache
  • upset stomach
  • redness and swelling of the neck
  • heart palpitations
  • sweating
  • chills

Bile acid-binding resin

Resins help your body break down LDL cholesterol. Your body uses cholesterol to make bile, which is used in the digestive process. As the name implies, this type of medicine binds to bile. This prevents bile from being absorbed during digestion. The body responds by producing more bile, which requires more cholesterol. The more bile is produced, the more cholesterol the body will use. This reduces the amount of cholesterol in the blood. Here are some examples of bile acid-binding resins

  • Cholestyramine (Locorest, Prevalite, Questran)
  • Colesevelam

These drugs should be avoided by people with liver or gallbladder problems. Side effects may include the following

  • Constipation
  • Gas
  • Heartburn
  • Indigestion
  • Nausea

Cholesterol Absorption Inhibitors

Selective cholesterol absorption inhibitors help lower LDL cholesterol by preventing LDL cholesterol from being absorbed in the intestine. They also help increase HDL cholesterol. The first drug in this class, ezetimibe (Zetia), was approved in 2002. These drugs should not be taken by people with liver disease. Side effects may include the following

  • stomach pain
  • fatigue
  • joint pain
  • diarrhea
  • Dizziness
  • Headache
  • Sore throat
  • Runny nose
  • Sneezing


Fiber-based medications can be used alone or in combination with other medications. They can help improve cholesterol in the diet.

Do not use Fibrate if you have kidney problems or gallbladder or liver problems. Some side effects may include

  • constipation
  • diarrhea
  • dizziness
  • headache
  • stomach pain

Note: When taken with statins, fiber may increase the risk of muscle problems.

Omega-3 fatty acids (fish oil)

If your blood triglyceride levels are very high (over 500 ml/dL), you can use a prescription omega-3 fatty acid called Lovaza. Omega-3 fatty acids are also available as supplements but at lower doses. Some side effects include the following

  • Back pain
  • Excretion
  • Flu symptoms
  • Stomach pain
  • confusion
  • Increased risk of infection


Niacin, also known as vitamin B-3, can help improve cholesterol by raising HDL and lowering LDL and triglyceride levels. When used in combination with statins, niacin can increase HDL levels by more than 30%. Niacin can be purchased without a prescription, but over-the-counter doses are not effective in treating high cholesterol. Because of the side effects of niacin, it is now generally reserved for people who cannot tolerate statin therapy.

Here are a few examples of niacin prescriptions

  • Niacor
  • Niaspan
  • Slow niacin

Niacin should be avoided by people with diabetes because it can raise blood sugar levels. Other side effects that may occur include

  • Redness in the neck
  • Nausea
  • Vomiting
  • diarrhea
  • Jaundice
  • Elevated liver enzyme levels
  • Gastrointestinal ulcers
  • Itching
  • Numbness in the feet

PCSK9 inhibitors

PCSK9 inhibitors are monoclonal antibodies, which are a type of biological drug. They are a new class of drugs used to treat patients with high cholesterol.PCSK9 inhibitors help lower cholesterol by targeting and inactivating a protein called proprotein convertase subtilisin ketone 9. This protein reduces the number of receptors on the liver that remove LDL cholesterol from the blood; when PCSK9 is inactivated by PCSK9 inhibitors, more receptors are available to remove LDL cholesterol from the blood. As a result, cholesterol levels are lowered. These drugs complement other treatments for more severe hypercholesterolemic conditions, such as familial hypercholesterolemia.

In 2015, the U.S. Food and Drug Administration (FDA) approved the first PCSK9 inhibitors. They are Praluent (alirocumab) and Repatha (evolocumab). Both are injectable drugs that can be used to treat people who are unable to lower their cholesterol with other drugs. Studies have shown that these two PCSK9 inhibitors are very effective in lowering cholesterol levels and improving overall health.

However, like all drugs, PCSK9 inhibitors have their drawbacks. Pruent and Rebalta require injections every two to four weeks. This can be uncomfortable for many people. These drugs are also expensive, with some officials estimating that a year’s worth of treatment could cost as much as $12,000.

PCSK9 inhibitors may also cause side effects in some people, including

  • Itching, swelling, pain, or bruising at the injection site
  • Back pain
  • confusion
  • fogginess or confusion
  • cold or flu
  • Wind chill
  • Allergic reactions, such as boils or hives


Most medications can lower cholesterol without causing serious side effects. However, each medication works differently for each person. You and your doctor will need to decide which type of medication is best for you. Remember to tell your doctor about any other medications you are taking, as some may interfere with the effects of cholesterol-lowering medications.

Once you receive your prescription, be sure to take your medication exactly as directed. If you experience any side effects, tell your doctor. Your doctor may tell you to take a different medication or reduce your dose. Never stop taking your medication unless your doctor tells you to.