Drugs to Treat Cholesterol, How They Act, Side Effects and Examples

If your high cholesterol has warranted treatment, it may be due to three reasons:

or

  • You have high LDL cholesterol levels and you are also a high-risk patient for heart attack and stroke.

But, if you have been faithfully following the advice given in the above two posts and yet have not been able to lower cholesterol level in three months to six months, then you have a very “stubborn cholesterol”, which has then to be lowered through treatment with medications.

Secondly, even otherwise if your doctor feels that you are at a high risk of a heart attack or stroke by judging your risk factors, he would want to start the medication immediately without giving you a chance first to lower your cholesterol through diet, lifestyle, and exercise alone.

These risk factors could be a pre-existing heart condition, or/and diabetes, high blood pressure or morbid obesity.

Criteria for cholesterol medication: Indications

The following are the criteria for putting a patient with high cholesterol on medication:

  • A patient whose raised cholesterol could not be lowered with “Therapeutic Lifestyle Changes” (TLC), which include the proper diet, regular exercise, and good lifestyle practices.
  • An adult with high cholesterol and heart disease, risk factors such as long-standing high blood pressure, diabetes, heavy family history, morbid obesity, etc.
  • A person with a history of cardiovascular disease such as heart attack, stroke, angina, peripheral vascular disease, transient ischemic attack.
  • Any person, 21 years and older with very high LDL cholesterol of around 190 mg/dL
  • Any diabetic, 45 years and older with raised LDL cholesterol.

There are several prescription drug options available and your doctor is the best person to choose the cholesterol medication that effectively suits you.

However, after starting cholesterol treatment, it is still imperative that you follow the prescribed diet and the lifestyle changes in which exercise, especially aerobics, play a very important part. Both diet and lifestyle changes are to be considered as part of the treatment along with the cholesterol medicines.

The aim is to keep your cholesterol levels within the normal limits with the least required dose

Any of the following doctors or specialists can order a cholesterol test and advise treatment.

  • Family medicine doctor
  • Internal medicine doctor
  • Cardiologist.

A word of caution:

According to the University of Maryland Medical Center, vitamin D should not be taken at the same time as cholesterol-lowering drugs because it can cause the drug to be less effective.

Guidelines for starting cholesterol treatment with drugs

There are various guidelines advocated for the treatment of cholesterol.

NCBI gives a detailed informative chart of comparison.

How often should you test for cholesterol?

Having high cholesterol is like having diabetes and hypertension. These disorders usually do not announce themselves with symptoms. At times, you go the doctor after their complications set in such as a heart attack or a stroke. That is why they fall under the “silent killers” category.

If you are an otherwise healthy individual not aware of your chemistry panel and above the age of 35 years, you should know how often you should test for cholesterol.

If your high cholesterol levels have been detected, you should test for cholesterol every three months whether you are on the “therapeutic lifestyle changes” (TLC) regimen or on medications.

Once your normal levels have been established and the dose of your medication finalized, you should test every year to confirm your normal levels.

Cholesterol treatment goals

That your doctor is starting you on medication is indication enough that you are at a high risk for coronary heart disease. The basic aim that guides the cholesterol therapy is to bring down the LDL cholesterol levels below 100 mg/dL.

Thereafter, the emphasis shifts to managing the other risk factors that have raised your cholesterol such as metabolic syndrome, which can include diabetes, obesity and more.

TLC plays an important role in controlling your risk factors and forms part of your treatment and management.

Cholesterol drugs, mechanism of action, side effects & examples with brand names

Therapy with statins and other drugs can have a dramatic lipid lowering effect on your blood levels.

There are various factors that influence the choice of drugs or their combinations such as individual risk factors, age, your current health status and the possibility of developing side effects.

Cholesterol medications do have their side effects and give the impression of being bad, but these side effects are not common and the benefits of lowering cholesterol far outweigh the risks of their side effects.

Secondly, in the event of side effects such as liver damage due to statins, there are several other drug options besides statins and combinations available that your doctor can prescribe.

Here is the list of cholesterol lowering medications with their mode of action, their side effects and examples with their generic and brand names. You should know that treatment once started has to be continued throughout life.

Statins are the most preferred drugs to treat high cholesterol. However, non-statins alternative options are also available along with some newly found drugs, which efficiently lower your cholesterol.

Statins

Statins are the most preferred and effective of the cholesterol reducing medicines. They lower LDL cholesterol by 30 to 55%. They also modestly reduce triglycerides and slightly increase HDL.

You should read this post on the statins, which describes their mode of action, side effects, precautions to follow, and examples with brand names.

Bile acid sequestrants or resins

Mechanism of action

Resins lower LDL by binding themselves with bile acids, which contain cholesterol and inhibiting their absorption. Being a major component of bile acids, cholesterol plays an important part in their production.

Resins promote excretion of these bile acids through the intestine, thereby helping in getting rid of cholesterol.

As a result, more cholesterol is drawn from the blood to make bile acids, which again, resins help to excrete. This is how resins help to reduce cholesterol. They reduce LDL by 15 to 25%, slightly raise VLDL and triglycerides and have minimal action on HDL levels

The cholesterol reducing action of resins is not very strong and they are sometimes given in conjunction with statins.

Side effects of bile acid sequestrants or resins

  • Constipation
  • Gas
  • Dyspepsia
  • Low vitamin D levels

Examples of bile acid sequestrants or resins

  • Cholestyramine (Brand name Questran)
  • Colestipol (Colestid)
  • Colesevalam (Welchol).

Cholesterol absorption inhibitors

Cholesterol absorption inhibitors lower LDL cholesterol blood levels by 15 to 25%. They have a minimal effect on HDL.

They are not as effective as statins in reducing cholesterol but when administered along with them, they greatly enhance the action of statins and reduce the risk of cardiac events.

Mode of action

As the name suggests, they act directly by reducing the absorption of cholesterol from the intestines.

Examples

Ezetimibe (Brand name Zetia)

Side Effects 

Side effects are rare and include edema or swelling of the tongue, which is called angioedema. Ezetimibe (Zetia) can cause muscular back pain, pain in the abdomen, and diarrhea.

Fibrates (also called fibric acid derivatives)

Mechanism of action

Fibrates act by stimulating the extra production of an enzyme, which breaks down the fats in the blood.

They mainly reduce the triglycerides production in the body by 25-35% and marginally increase the HDL or the good cholesterol levels. They are not very useful in lowering LDL levels.

Examples of Fibrates

  • Gemfibrozil (Lopid)
  • Fenofibrate (Tricor)
  • Clofibrate (Atromid-S)

Side Effects

Side effects include gastrointestinal symptoms like flatulence and nausea. Fibrates increase the likely hood of gallstone formation. If a patient is on anticoagulation therapy, fibrates increase the action of the anticoagulants causing thinning of the blood.

Such a combined therapy of fibrates and anticoagulants requires strict medical supervision as it can give rise to bleeding either in the gastrointestinal tract or the urinary tract or from an injury.

Niacin or Nicotinic acid

Niacin is a B vitamin and is also referred to as nicotinic acid. It is used for cholesterol treatment and differs from the over-the-counter Niacin ( Nicotinamide) of  Vitamin B’ complex, which has no role in treating high cholesterol.

Niacin lowers LDL, the bad cholesterol by 5 to 20% and the triglycerides and effectively raises HDL, the good cholesterol. However, high doses are required.

They are available as short-acting or immediate release and long acting or extended release.

Examples

  • Niaspan
  • Nicoar
  • Advicor is available in combination of Niacin with Lovastatin

Side Effects

Side effects include hot flushes, gastrointestinal symptoms like nausea, vomiting, diarrhea and indigestion. Long-term treatment can cause peptic ulcer, liver toxicity, gout and increased blood sugar levels.

PCSK9 Inhibitors: The latest addition

These drugs are used in stubborn cases where the cholesterol is not controlled through the use of lifestyle changes and statins.

Mode of action

They inhibit the action of the protein PCSK9 to destroy the LDL receptors due to which the body is easily able to get rid of LDL from the blood.

They are mainly advocated for those cholesterol patients who have their levels raised due to a genetic factor. This condition is called heterozygous familial hypercholesterolemia and is difficult to treat.

This drug is given as an intramuscular shot every two weeks

Examples include

  • Alirocumab (Praluent)
  • Evolocumab (Repatha)

Side effects

As of now, side effects identified include itching, swelling, pain, at the site of the injection, colds, and flu.

Action Step: As stated above, always consult your doctor on any issue regarding cholesterol treatment and do follow up with regular blood tests for cholesterol. It may sometimes be necessary over time for your doctor to alter the cholesterol medicines or their dosage.

 

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