Drugs for Cholesterol

Cholesterol is a fat found in the blood. It’s produced by the liver and found in foods from animal sources, such as meat, poultry, and full-fat dairy products. The body needs some cholesterol to ensure organs grow and function properly. However, too much cholesterol in the blood can clog the arteries and lead to serious health conditions.

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 helps remove cholesterol from the blood vessels and carries it back to the liver, where it’s eliminated from the body through urination. LDL, on the other hand, is considered the “bad” type of cholesterol. It can cling to the blood vessels and block blood flow. This blockage makes the heart work much harder than it should. People with high levels of LDL are therefore at an increased risk for heart disease, heart attack, and stroke. This is why it’s critical to lower the amount of LDL in the blood.

Making healthy eating choices and increasing exercise are usually the first steps in improving cholesterol. However, diet and lifestyle adjustments alone may prove ineffective for some. In these cases, doctors may recommend using medications that either lower LDL cholesterol or raise HDL cholesterol. Here’s a breakdown of some of the drugs that can be used to treat high cholesterol.

Statins

Statins decrease the production of cholesterol in the liver and help remove excess cholesterol from the blood vessels. While statins are very effective in lowering LDL cholesterol levels, they only slightly improve levels of HDL cholesterol. Examples of statins include:

  • atorvastatin (Lipitor)
  • fluvastatin (Lescol)
  • lovastatin (Altoprev and Mevacor)
  • pitavastatin (Livalo)
  • pravastatin (Pravachol)
  • rosuvastatin Calcium (Crestor)
  • simvastatin (Zocor)

Avoid taking statins if you have liver disease or if you’re pregnant. You should also avoid drinking grapefruit juice while taking this medication.

Side effects of statins include:

  • constipation
  • diarrhea
  • dizziness
  • gas
  • headache
  • upset stomach
  • muscle pain

Statins can also be found in medications that combine other cholesterol-lowering drugs for additional benefits. These include:

  • lovastatin with niacin (Advicor)
  • simvastatin with ezetimibe (Vytorin)
  • atorvastatin with amlodipine (Caduet)

You shouldn’t take Vytorin or Advicor if you’re pregnant or breast-feeding or if you have liver disease. As with statins, don’t drink grapefruit juice while taking these combination medications. Side effects may include:

  • headache
  • upset stomach
  • facial and neck flushing (redness)
  • heart palpitations
  • sweating
  • chills

Bile-Acid-Binding Resins

Resins help the body dispose of LDL cholesterol. Your body uses cholesterol to create bile, which is used in the digestive process. As the name suggests, this class of drugs binds to bile. This prevents bile from being absorbed during digestion. The body responds by making even more bile, which requires more cholesterol. The more bile it makes, the more cholesterol the body uses. This lowers the amount of cholesterol in your bloodstream. Examples of bile-acid-binding resins include:

  • cholestyramine (Locholest, Prevalite, and Questran)
  • colesevelam (Welchol)
  • colestipol (Colestid)

People with liver or gallbladder problems should avoid using these medications. Side effects may include:

  • constipation
  • gas
  • heartburn
  • indigestion
  • nausea

Selective Cholesterol Absorption Inhibitors

Selective cholesterol absorption inhibitors help lower LDL cholesterol by preventing its absorption by the intestines. They may have a modest effect on boosting HDL cholesterol as well. The first medication of this class, ezetimibe (Zetia), was first approved in 2002. People with liver disease shouldn’t take this type of medication. Side effects may include:

  • stomach pain
  • fatigue
  • joint pain
  • diarrhea
  • dizziness
  • headache
  • sore throat
  • runny nose
  • sneezing

Fibrates 

Fibrates may be used alone or in combination with other drugs. They help improve cholesterol by lowering triglycerides and raising HDL cholesterol. Examples of fibrates include:

  • clofibrate (Atromid-S)
  • gemfibrozil (Lopid)
  • fenofibrate (Antara, Lofibra, and Triglide)

People with kidney problems, gallbladder disease, or liver disease shouldn’t use fibrates. Side effects may include:

  • constipation
  • diarrhea
  • dizziness
  • headache
  • stomach pain

Note: When taken with statins, fibrates may increase the chance of muscle problems.

Omega-3 Fatty Acid (Fish Oil)

A prescription-strength omega-3 fatty acid called Lovaza can be used for the treatment of very high blood triglycerides (above 500 ml/dL). Omega-3 fatty acids are also available as supplements, but in lower doses. Side effects may include:

  • back pain
  • burping
  • flu-like symptoms
  • upset stomach
  • skin rash
  • increased risk for infections

Niacin (Nicotinic Acid)

Prescription-strength niacin, also known as vitamin B-3, may help improve cholesterol by boosting HDL and lowering LDL and triglyceride levels. When used in combination with statins, niacin could raise HDL levels by 30 percent or more. Although you can buy niacin without a prescription, over-the-counter doses aren’t effective in treating high cholesterol. Due to side effects, niacin is now usually reserved for those who can’t tolerate statin therapy.

Examples of prescription-strength niacin include:

  • Niacor
  • Niaspan
  • Slo-Niacin

People with diabetes should avoid taking niacin, as the medication may increase blood sugar levels. Other side effects may include:

  • facial and neck flushing
  • nausea
  • vomiting
  • diarrhea
  • jaundice (yellowing of  the eyes or skin)
  • increased levels of liver enzymes (found with a blood test)
  • peptic ulcers
  • itching
  • tingling sensation in the legs and feet

PCSK9 Inhibitors

PCSK9 inhibitors are monoclonal antibodies, a type of biologic drug. These medications are a new class of drug being used to treat people who have high cholesterol. They help lower cholesterol by targeting and inactivating a protein called proprotein convertase subtilisin kexin 9. This particular protein reduces the number of receptors on the liver that remove LDL cholesterol from the blood. When PCSK9 is deactivated by a PCSK9 inhibitor, there are more receptors available to eliminate LDL cholesterol from the blood. As a result, cholesterol levels drop. These drugs are added to other treatments, for the most severe high cholesterol conditions, like familial hypercholesterolemia.

In 2015, the U.S. Food and Drug Administration (FDA) approved the first PCSK9 inhibitors: Praluent (alirocumab) and Repatha (evolocumab). Both are injections that may be used to treat people who are unable to lower their cholesterol using other medications. Studies show that both PCSK9 inhibitors are very effective in lowering cholesterol levels and improving overall health.

Like all medications, however, PCSK9 inhibitors do have their downsides. Both Praluent and Repatha need to be injected every two to four weeks. This can be inconvenient for many people. These medications are also expensive, with some officials estimating that a year’s worth of treatment could cost up to $12,000.

PCSK9 inhibitors can also cause side effects in some people, including:

  • itching, swelling, pain, or bruising at the injection site
  • back pain
  • confusion
  • difficulty concentration
  • the common cold
  • the flu
  • allergic reactions, such as rash and hives

The Takeaway

Most medications can lower cholesterol without causing serious side effects. But the effectiveness of each medication varies from person to person. You and your doctor will need to determine which class of medication is right for you. Make sure to notify your doctor about any other medications you’re currently taking, as certain drugs can interfere with the effectiveness of cholesterol-lowering medicines.

Once you’ve received your prescription, it’s important for you to take your medication exactly as directed. Let your doctor know if you experience any side effects. Your doctor may switch you to another medication or reduce your dosage. Never stop taking your medication unless your doctor instructs you to do so.