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High Cholesterol Drugs

Written by the Healthline Editorial Team | Published on October 20, 2014
Medically Reviewed by Kenneth R. Hirsch, MD on October 20, 2014

High Cholesterol Treatments

Unless your cholesterol is at a dangerous level, lifestyle changes are often recommended as the first line of treatment. Your lifestyle is what you can control to help keep your cholesterol levels healthy. Medications can also help lower cholesterol. For some people, diet and exercise alone can treat high cholesterol. Others may have to rely on a combination of lifestyle changes and medication to get their cholesterol down to a healthier level.

Healthy Diet

Dietary modifications combined with weight loss can lower “bad” LDL (low-density lipoprotein) cholesterol. A heart-healthy diet promotes fruits, vegetables, whole grains, and legumes. It limits intake of sugar, sodium, and saturated fat. Anything that contains hydrogenated oil also contains trans fat and should be avoided. What sets heart-healthy diets apart from others is the emphasis on good fats, such as those found in fish, nuts, olive oil, avocados, and seeds. When used in place of saturated and trans fats, these oils (polyunsaturated and monounsaturated fats) can help reduce cholesterol. According to the Harvard Medical School, some research also indicates that avoiding refined carbohydrates may boost “good” HDL (high-density lipoprotein) cholesterol and lower triglycerides. Refined carbohydrates include white rice, white bread, soft drinks, and some baked goods.

Weight Loss

People who are obese (a body mass index more than 30) tend to have lower HDL cholesterol and higher LDL cholesterol and triglycerides than people of normal weight. Whether you are obese or simply overweight, losing weight can improve your cholesterol.

Avoid or Quit Smoking

Smoking damages your blood vessels and speeds up the hardening of the arteries. According to the Centers for Disease Control and Prevention (CDC), it greatly increases your risk for heart disease, including high cholesterol.

Exercise

Being inactive can elevate LDL cholesterol. Exercise can help lower it. Moderate activity like brisk walking can also help lower triglycerides. Vigorous exercise like running can boost HDL cholesterol. Cardiovascular exercise can also strengthen your heart and reduce blood pressure, which is a major risk factor for stroke.

Medication

Your doctor may also recommend medication to manage your cholesterol. Drug therapy generally tends to affect cholesterol levels more quickly than diet and exercise. Your doctor may prescribe medication if they feel it’s important to get your cholesterol down immediately.

There are many different drugs used to treat cholesterol issues. They can either lower LDL cholesterol, raise HDL cholesterol, or both. Your doctor can decide which drug is right for your condition. Tell your doctor about any other medications (including herbs and supplements) you take. They may not interact well with cholesterol-modifying drugs.

Take your cholesterol medication exactly as directed. Tell your doctor right away if you have any unpleasant side effects. Cholesterol drugs can be very effective, but you should also adopt a heart-healthy diet and exercise program to achieve the best results.

Statins

Statins are some of the most commonly used drugs to treat cholesterol problems. Statins are HMG-CoA reductase inhibitors. They slow down the body’s production of cholesterol. They also help to eliminate some of the excess cholesterol from your arteries. Statins are primarily used to lower LDL cholesterol levels. In some cases they can slightly improve triglyceride and HDL cholesterol levels. For people who have already suffered a heart attack, starting a statin medication lowers their risk of a second heart attack, stroke, or death. Many different practice guidelines advocate the use of statins in patients with cholesterol problems, but it remains controversial as to whether or not statin treatment lowers the risk of death in people who have never had a heart attack or stroke.

You should not drink grapefruit juice when taking your statin medication. Grapefruit juice and other citrus fruits and juices can interfere with certain enzymes that help breakdown medications in your digestive system. This can increase the potency of the medication and cause potentially dangerous side effects. Talk to your doctor before taking statins if you are pregnant, breast-feeding, or have any liver conditions.

Some of the most common statin drugs and their brand names include:

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

Some possible side effects of statins include:

  • constipation
  • diarrhea
  • dizziness
  • intestinal gas
  • headache
  • upset stomach
  • sore muscles
  • liver damage

Combination Statins

Some statin medications contain an additional drug to help lower triglycerides or boost HDL cholesterol. They include:

  • atorvastatin with amlodipine (Caduet) – works to decrease blood pressure and treat angina
  • lovastatin with niacin (Advicor)
  • simvastatin with ezetimibe (Vytorin)

Side effects of combination statins generally have the same side effects as other statins. Talk to your doctor if you have any concerns about possible side effects.

Bile Acid-Binding Resins

Also called bile acid sequestrants, these drugs help the body dispose of cholesterol. Your body uses cholesterol to create the bile used to digest food. These drugs bind to bile so that it can’t be used. The liver is then required to use more cholesterol in order to make additional bile. This lowers the total level of cholesterol that reaches your bloodstream.

These drugs are sometimes prescribed in addition to statins for people with very high cholesterol. People with liver or gallbladder problems should avoid these medications. Examples of bile-acid-binding resins include:

  • cholestyramine (Locholest, Locholest Light, Prevalite, Questran, Questran Light)
  • colesevelam Hcl (WelChol)
  • colestipol (Colestid)

Side effects may include:

  • constipation
  • intestinal 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. People with liver disease should not take this type of medication. An example of this type of cholesterol drug is ezetimibe (Zetia).

Side effects may include:

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

Fibrates 

Used alone or in combination with other drugs, fibrates work by lowering triglycerides. In some cases they can raise “good” HDL cholesterol. People with kidney problems, gallbladder disease, or liver disease should not use fibrates. Examples of fibrates include:

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

Side effects may include:

  • constipation
  • diarrhea
  • dizziness
  • headache
  • stomach pain

When taken with a statin, fibrates may increase the chance of a very serious side effect whose symptoms include muscle pain or weakness.

Omega-3 Fatty Acid (Fish Oil)

A prescription-strength fish oil (omega-3 fatty acid) called Lovaza is FDA-approved for the treatment of very high blood triglycerides (above 500 milligrams per deciliter (mg/dL)). Omega-3 fatty acids are also available as supplements, but in lower doses.

Some possible side effects may include:

  • back pain
  • burping
  • flu-like symptoms
  • taste changes
  • upset stomach
  • skin rash
  • increased risk of infections

Niacin (Nicotinic Acid)

Prescription-strength niacin (vitamin B3) can boost HDL cholesterol and lower LDL cholesterol and triglyceride levels. When used in combination with statins, niacin could raise HDL cholesterol levels significantly. Although you can buy niacin without a prescription, over-the-counter formulations (doses) are not effective in treating high cholesterol. Examples of prescription-strength niacin include:

  • Niacor
  • Niaspan
  • Slo-Niacin

Don’t take high doses of niacin without a prescription from your physician. It may can harmful side effects and increase blood glucose levels in people with diabetes.

Side effects may include:

  • flushing
  • headache
  • itching
  • tingling sensation in extremities
  • upset stomach

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