Cholesterol Basics

Cholesterol Basics

What is cholesterol?
Cholesterol is a soft, fatlike, waxy substance that is found in the bloodstream and in the body’s
cells. It is found in the family of lipids along with fat. The body needs a certain amount of
cholesterol to aid in the formation and maintenance of cell membranes to help the body resist
changes in temperatures and protect and insulate nerve fibers. Cholesterol is also used in the
production of normal sex hormones in the body including progesterone, testosterone, estradiol,
and cortisone. Also, it produces bile salts, which help in digestion, and converts vitamin D in the
skin when it is exposed to sunlight.
Although everyone needs cholesterol for normal body functions, too much cholesterol can lead
to cardiovascular disease, which can result in a heart attack. Cholesterol and fat cannot travel
through the body in their original form because they do not mix with water, the main component
of blood. Cholesterol and fat are grouped with proteins to make lipoproteins, which travel
through the blood. There are three types of lipoproteins: low-density lipoproteins (LDL), high-
density lipoproteins (HDL), and very low-density lipoproteins (VLDL).

LDL is known as “bad” cholesterol. Having too much LDL can cause some cholesterol to stick
to blood vessels forming plaques; these are thick, hard deposits that can cause arteries to clog.
This condition is called atherosclerosis, and it can lead to a heart attack or stroke.

HDL is known as “good” cholesterol because it picks up the LDL cholesterol that sticks to the
blood vessel walls and takes it back to the liver where it is eventually eliminated out of the body.

VLDLs are made in the liver to carry fat to other parts of the body. The leftover pieces change
into LDL.

Triglycerides are also important. They are a form of fat found in the blood. Triglycerides come
from fats in foods or are made in the body from energy sources like carbohydrates. Calories
eaten during a meal that are not used immediately by tissues are converted to triglycerides and
transported to fat cells to be stored. Having elevated triglycerides can also be a complication due
to diabetes.



Where does cholesterol come from?

One gets cholesterol through two ways. The body makes some in the liver to keep the cells
working; the rest comes from foods. Foods high in cholesterol include fatty meats, poultry, fish,
eggs, butter, cheese, and whole milk. Foods high in saturated fat can allow the body to
overproduce cholesterol.

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What happens to the cholesterol in the diet?

After the high-fat foods are ingested, the fat passes through the stomach and small intestine and
is sent to the liver. The liver changes fat and cholesterol into VLDLs that travel through the
blood vessels unloading the fat; the remainder becomes LDLs. LDL cholesterol travels through
the blood vessels and some sticks to the vessel walls. HDL picks up the stuck cholesterol and
brings it back to the liver where they are made into new VLDLs or broken down and eliminated
out of the body.

If one eats too much fat, the liver will make extra VLDLs, which eventually become LDLs.
Therefore, more of the cholesterol is left in the blood vessels making them narrower. If there is
not enough HDL to pick up the LDLs, the blood vessels can become blocked.

How often should cholesterol be checked?

Adults age 20 or over should have a fasting cholesterol profile once every 5 years. A fasting
profile means that no food has been eaten in the past 9 to 12 hours. A blood sample is taken and
analyzed by a laboratory. If a patient is nonfasting, only total cholesterol and HDL can be
evaluated. If total cholesterol is equal to or more than 200 mg/dL or HDL is less than 40 mg/dL,
a fasting cholesterol profile is needed to decide on appropriate therapy. If values are abnormal
or if certain medical problems such as type 2 diabetes are present, more frequent testing is
recommended. There are separate values and considerations for adolescents.

What are the numbers?

The current values for cholesterol levels are as follows:
• LDL (“bad” cholesterol) The higher the number of LDLs, the more likely cholesterol is
beginning to stick to the blood vessels.


less than 100: optimal

100 to 129: near optimal

130 to 159: borderline high
160 to 189: high
equal to or more than 190: very high

• Total cholesterol—the sum of VLDL, LDL and HDL


less than 200: desirable
200 to 239: borderline high
equal to or more than 240: high

• HDL (“good” cholesterol) The higher the number, the better, since this means that the
HDL will help remove the cholesterol that is stuck to the blood vessels.


less than 40: low

more than 60: high (for HDL, high is good)

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• Triglycerides



less than 150: desirable

150 to 199: borderline high

equal to or more than 200: high

Treatment goals, however, are determined from an assessment of a person’s 10-year risk for
heart attack and certain other types of heart disease.

What affects cholesterol levels?

Lifestyle: Diet: Diets high in saturated fats and cholesterol can increase cholesterol
levels.
Weight: Being overweight can increase cholesterol levels. The body
stores more fat and cholesterol. It is also a risk factor for cardiovascular
disease regardless of cholesterol levels.
Exercise: Not exercising is a risk factor for cardiovascular disease.
Regular exercise can help lower LDL, raise HDL, and lower weight, thus
lowering heart disease risks.
Smoking:
Smoking lowers HDL cholesterol and increases the risk of a
heart attack and stroke, as well as cancer.

Heredity:
High cholesterol does run in families. Genes play a role in how much
cholesterol the body manufactures.

Gender:
Men typically have higher LDL and lower HDL levels than women of the
same age have. After a woman goes through menopause, her cholesterol
level usually rises.

Age:

As you age, cholesterol levels rise.

In addition, what are the risk factors for developing heart disease or having a heart attack?

Major risk factors:
• Cigarette smoking
• Hypertension (blood pressure equal to or higher than140/90 or taking antihypertensive
medication)
• Low HDL cholesterol (less than 40 mg/dL)
• Family history of heart disease (in males first degree relative younger than 55 years; in
females first degree relative younger than 65 years)
• Age (men 45 years or older; women 55 years or older)
Conditions that put one at high risk of heart disease:
• Peripheral arterial disease
• Abdominal aortic aneurysm
• Carotid artery disease (stroke, TIA)

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• Diabetes

Some patients have many risk factors that make up a condition called the metabolic syndrome.
These include abdominal obesity, elevated triglycerides, small type of LDL, low HDL, raised
blood pressure, and insulin resistance.

What are the current cholesterol goals?

LDL is the main component of cholesterol used to determine cholesterol goals. The cholesterol
goal is determined based on the number of patient risk factors as follows.

If a patient has coronary heart disease or any of the four conditions mentioned above that put him
or her at high risk of coronary heart disease
LDL goal is less than 100 mg/dL
If current LDL level is more than 130: need to start medication along with diet and
exercise
If current LDL level is 100 to 129: need to start diet and exercise and may also need
medication
If current LDL is less than 100: patient should still follow a diet and exercise plan

If a patient has two or more risk factors
LDL goal is less than 130 mg/dL

If current LDL is more than 160: need medication along with diet and exercise
If LDL level is 130 to159, need to start diet and exercise and may eventually need
medication

If a patient has zero to one risk factor
LDL goal is less than 160 mg/dL
If LDL is more than 190: need medication along with diet and exercise
If LDL is 160 to 189: need diet and exercise and may eventually need


medication

General guides for screening purposes:
HDL more than 40 mg/dL
Total cholesterol less than 200 mg/dL
Triglycerides less than 150 mg/dL

What can be done to help lower cholesterol and reduce the risk of coronary heart disease?

Make lifestyle changes
• Diet: Changing diet is often the most effective way to lower cholesterol or maintain
cholesterol at a healthy level. It may take a few months to see the results. Saturated fat
and cholesterol found in foods can increase cholesterol. Patients should reduce the
amount of saturated fat to less than 7 percent of their total calories and reduce cholesterol
to less than 200 mg per day. Foods low in saturated fat include low-fat or fat-free milks,
lean meats, fish, skinless chicken, whole grain foods, and fruits and vegetables. Intake of

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soluble fiber should also be increased every day. Sources of fiber include whole wheat
products, oats, potatoes, raw vegetables, raw fruits, and beans. Fiber helps lower
cholesterol by helping to keep the cholesterol eaten from being absorbed. Starches can
help lower cholesterol as well by diluting the amount of fat intake. Foods high in
starches include grains, beans, and root vegetables. Also, plant stanols can be added to
the diet to help lower cholesterol. Plant stanols are natural products found in plants.
They are combined with a small amount of canola oil to form stanol esters. Stanol esters
help block cholesterol absorption from the digestive tract. For example, Benecol, a
cholesterol-lowering margarine, contains plant stanols. The recommended serving is 3
squares each day in place of other butter or spreads. Alcohol should only be consumed in
moderation; too much can raise the fat levels in the blood.
• Lose weight: The more one weighs, the more the body stores fat and cholesterol. A good
way to lose weight is to reduce the amount of fat in the diet because it contains the most
calories.
• Exercise: Regular physical activity can help lower LDL and raise HDL. It can also help
one lose weight. The current recommendation is to exercise at least 30 minutes daily,
five times per week.
• Reduce other heart risks: Stop smoking, control high blood pressure or diabetes, and
reduce the amount of stress in life
• Get regular checkups: Visit with your doctor regularly to make sure cholesterol levels
are desirable and all other health risks are under control.

What medications are used to treat high cholesterol?

Currently, many classes of drugs are available to treat high cholesterol, and they all affect the
various components of cholesterol differently. The classes of agents are detailed below. HMG
CoA reductase inhibitors (commonly known as “statins”) are the most commonly prescribed
medications and are the most effective in lowering LDL levels. Bile acid sequestrants also help
lower LDL and are usually chosen along with a statin or if a patient cannot take a statin due to
side effects or other reasons that make this treatment inadvisable. Bile acid sequestrants may
raise triglycerides and should not be used in patients with elevated triglycerides. Fibric acid
derivatives are the main class to help lower triglycerides and also help lower LDL levels.
Nicotinic acid helps raise HDL and also lowers triglycerides. It has some effect on lowering
LDL levels. Ezetimibe is a new drug class that is used mainly to lower LDL. It is usually given
along with a statin when a statin alone is not effective in lowering LDL levels to goal. It can also
be used alone. Fish oils are available over-the-counter and are also found in certain types of fish.
The main effect is lowering triglycerides. It is very important to remember that medications are
supplements to the primary treatment, which is lifestyle modifications.


• HMG CoA reductase inhibitors (also known as Statins)
Lipitor
(atorvastatin)
Lescol
(fluvastatin)
Mevacor (lovastatin)
Pravachol (pravastatin)
Crestor (rosuvastatin)

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Zocor (simvastatin)

This is the most effective class of drugs for lowering LDL, the “bad” cholesterol. They inhibit
HMG CoA reductase, an enzyme that is the rate-limiting step in making cholesterol. Therefore,
they stop the “bad” cholesterol from being made in the liver. The statins are typically most
effective when taken at bedtime when most of the cholesterol is made in the liver. They also
help decrease triglycerides and increase HDL. Some of the statins have been shown to reduce
deaths from cardiovascular events. The main side effects one might experience are stomach
discomfort, muscle soreness, tenderness, weakness or pain, and possible abnormal liver function
tests. Patients should notify their doctors if they are experiencing any muscle symptoms or have
noticed brown urine. One should not be taking a statin if he or she has active or chronic liver
disease. After starting a statin, a blood test will need to be done after 12 weeks to make sure liver
function is normal.

• Bile Acid Sequestrants
Questran
(cholestyramine)
Colestid
(colestipol)
Welchol
(colesevelam)

The main use of this class of drugs is to lower LDL cholesterol. They act by binding bile acids
in the intestine through anion exchange. The binding results in a decrease of cholesterol in the
liver, which, in turn, lowers LDL cholesterol. The bile acid sequestrants also increase HDL but
have no effect on or may increase triglycerides. This class of medications has been shown to
reduce the risk of coronary events. The sequestrants are useful in combination with statins.
These medications should be used with caution in patients with high triglycerides because these
drugs can increase triglycerides. Patients with triglycerides (higher than 400 mg/dL) should not
receive the sequestrants, and it is recommended to avoid them if levels are higher than 250
mg/dL. Cholestyramine and colestipol are administered as powders that have to be mixed with
water or juice; colestipol is also available as a tablet. Colesevelam comes only in tablet form,
making it more convenient to administer and decreasing the risk of drug interactions.
Cholestyramine and colestipol can decrease the absorption of a number of drugs. It is generally
recommended to take the other drugs either one hour before or four hours after the
cholestryramine and colestipol. Colesevelam can generally be administered with other drugs.
The main side effects one might experience are constipation, bloating, indigestion, nausea,
abdominal pain, and belching.

• Fibric Acid Derivatives
Tricor
(fenofibrate)
Lopid
(gemfibrozil)

The fibric acid derivatives lower LDL and triglycerides and increase HDL. Fibric acids inhibit
lipolysis (the breakdown of fat) and decrease the amount of fatty acids taken up by the liver.
They also inhibit VLDL secretion by the liver, which results in a decrease in circulating VLDL
levels. They are most effective at lowering triglyceride levels. This class of medications has
been shown to reduce the risk of coronary events. They should not be used in patients with
severe liver or renal problems. The main side effects one might experience are heartburn,

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gallstones, muscle pain, weakness, soreness, and abdominal pain. It is recommended to take
fenofibrate with meals and gemfibrozil before meals. Patients should inform their doctors if they
are experiencing any type of muscle pain.


• Nicotinic Acid
Niacin (immediate release)
Niaspan (sustained release)
Nicobid (extended release)

Nicotinic acid works by inhibiting the production of VLDL by the liver. It inhibits the peripheral
mobilization of free fatty acids, reducing liver secretion of VLDL. This medication is most
effective at raising HDL, the “good” cholesterol. It decreases LDL and triglycerides as well.
Nicotinic acid is also known as vitamin B3, which is found in many foods including meat, eggs,
fish, cereal, milk, and green vegetables. The daily recommended dietary allowance of niacin is
14 to18 mg/day in adults. Small doses often increase HDL and decrease triglycerides, but doses
of 2 to 3 grams per day are often needed to lower LDL. Nicotinic acid has been shown to reduce
the risk of coronary events. The main side effects one might experience are flushing, itching, an
increase in blood sugar, gout due to increased uric acid, abdominal discomfort, heartburn,
diarrhea, vomiting, nausea, indigestion, and possible liver toxicity. Patients with liver disease
and severe gout should not receive nicotinic acid. Diabetics should be careful taking this
medication since it can raise blood sugar levels especially at higher doses. To minimize
flushing, the dose is usually started low and increased as one builds tolerance. After extended
use, most patients develop tolerance to the flushing. To reduce flushing, take a low dose aspirin
30 minutes to an hour before taking niacin. Niaspan and Nicobid are generally better tolerated
and do not cause as much flushing as niacin causes.

• Ezetimibe (Zetia)

This new class of cholesterol medication inhibits absorption of cholesterol from food. This
promotes elimination of cholesterol out of the body through the intestines before it can be
absorbed. It decreases LDL and triglycerides and increases HDL. It has the most effect when
given in combination with a statin. It can be taken with or without meals. The main side effects
include abdominal pain, diarrhea, chest pain, dizziness, headache, fatigue, and muscle pain.
Patients should tell their doctors if they experience any of these symptoms for a long time. It has
not yet been proven to reduce the risk of coronary events.

• Fish Oils

Fish oil capsules can be taken to help lower cholesterol. Fish oil is effective at lowering
triglycerides. Eating fish that contains fish oils, including mackerel, herring, tuna, halibut,
salmon, cod liver, or whale or seal blubber, can also help lower triglycerides. Fish oils contain
omega-3 fatty acids that can help lower cholesterol, blood pressure, and plaque formation. Fish
oils also can help reduce cardiac arrhythmia and arthritis pain as well as benefiting some cancer
treatments. The most common side effects are fishy taste, bad breath, heartburn, and upset
stomach. Patients should talk to their doctors before trying fish oil capsules. Evidence has
shown that high intakes of omega-3 fatty acids (1 to 2 grams per day) can reduce the risk of

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major coronary events in patients who already have coronary heart disease. They may also
increase the risk of bleeding when given to patients on medications to prevent or reduce clotting.


Summary

Cholesterol numbers are important to watch, particularly as you age. Although some factors are
beyond our control since we are born with them, many factors can be addressed. Fortunately,
many effective medication options that will help prevent heart problems are available. The best
first defense, however, is to take charge of your own health through education, diet, and exercise.


References:
1. What’s the difference between LDL and HDL cholesterol? American Heart Association.
Dallas, TX. www.americanheart.org. 2002. Accessed January 6, 2004.
2. You can control your cholesterol: a guide to low-cholesterol living. San Bruno: The
Staywell Company for Merck & Co., Inc.; 2000.
3. Gordon, Jerry. How cholesterol works. How Stuff Works, Inc. Atlanta, GA.
http://health.howstuffworks.com/cholesterol1.html. 2004. Accessed January 26, 2004.
4. Triglycerides. American Heart Association. Dallas, TX. www.americanheart.org. 2002.
Accessed January 14, 2004.
5. Expert panel on detection, evaluation, and treatment of high blood cholesterol in adults.
Executive summary of the third report of the National Cholesterol Education Program
(adult treatment panel III). JAMA 2001; 285:2486-97.
6. High blood cholesterol: what you need to know. National Heart, Lung, and Blood
Institute (NHLBI) Information Center. Bethesda, MD. May 2001. Accessed January 6,
2004. http://www.nhlbi.nih.gov/health/public/heart/chol/wyntk.pdf also
http://www.nhlbi.nih.gov/guidelines/cholesterol/atglance.pdf
7. Plant stanol esters…another tool for lowering cholesterol. American Dietetic Association.
www.eatingright.org. 2003. Accessed January 30, 2004.
8. Expert panel on detection, evaluation, and treatment of high blood cholesterol in adults.
Final report of the third report of the National Cholesterol Education Program (adult
treatment panel III). National Institutes of Health and National Heart, Lung, and Blood
Institute. Bethesda, MD. http://www.nhlbi.nih.gov/guideline/cholesterol November 19,
2002. Accessed January 6, 2004.
9. Jellin JM, Gregory PJ, Scott GN, editors. Natural Medicines Comprehensive Database.
Stockton: Therapeutics Research Faculty; 2004.
10. Zetia [package insert]. Kenilworth, NJ: Merck/Schering-Plough Pharmaceuticals. March
2003.

Julie Jespersen, P4 Pharm.D. Candidate
Auburn University, Harrison School of Pharmacy

Bernie R. Olin, Pharm.D.
Director, Drug Information and Clinical Associate Professor
Auburn University, Harrison School of Pharmacy

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Reviewer
Pamela Stamm, Pharm.D.
Associate Professor
Auburn University, Harrison School of Pharmacy



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