Cholesterol is a waxy, fat-like substance made in the liver and other cells. It’s also found in certain foods, such as dairy products, eggs, and meat.

Your body needs some cholesterol to function properly.

Its cell walls, also known as membranes, need cholesterol to produce hormones, vitamin D, and the bile acids that help you digest fat. But the body only needs a limited amount of cholesterol. When there’s too much, health problems, such as heart disease, may develop.

Cholesterol travels through the blood attached to a protein.

The combination protein and cholesterol is called a lipoprotein.

There are three types of lipoproteins in your blood: high density, low

density, and very low density.

The specific type depends on how much protein there is in relation

to fat.

Low density lipoproteins (LDL) are also called "bad" cholesterol

because it can cause plaque buildup on the walls of arteries. The more LDL there is in the blood, the greater the risk of heart disease.

High density lipoproteins (HDL) are also called "good" cholesterol. It helps the body get rid of LDL. Maintaining a higher level of HDL is good. If your HDL level is low your risk of heart disease goes up.

Very low density lipoproteins (VLDL) are similar to LDL in that it contains mostly fat and not much protein.

Triglycerides, another type of fat, are carried in the blood by VLDL. Excess calories, alcohol, or sugar in your body are converted into triglycerides and stored in fat cells throughout your body.

DIET

Saturated fat and cholesterol in the food you eat increase

cholesterol levels. To lower your cholesterol level, try to

reduce the saturated fat and cholesterol in your diet.

WEIGHT In addition to being a risk factor for heart disease, being overweight can also increase cholesterol. Losing weight can help lower your LDL and total cholesterol. And it can also increase the level of HDL.

EXERCISE

Regular exercise can lower LDL and raise HDL. You should try to be

physically active for at least 30 minutes on most days.

AGE AND GENDER

As you get older, cholesterol levels rise. Before menopause, women

tend to have lower total cholesterol levels than men. After

menopause, though, women's LDL levels tend to rise.

DIABETES

Poorly controlled diabetes increases cholesterol levels. Having

control of your diabetes can cause your cholesterol levels to fall.

HEREDITY

Your genes partly determine how much cholesterol your body

makes. High blood cholesterol can run in families.

OTHER FACTORS

Certain medications and medical conditions can cause high

cholesterol.

High cholesterol, also known as hypercholesterolemia, is a major risk

factor for heart disease and stroke.

Abnormal levels of LDL cholesterol or HDL cholesterol are treated

with a low-fat diet, exercise, and medications such as statins.

High cholesterol is associated with an elevated risk of cardiovascular disease. That can include coronary heart disease, stroke, and peripheral vascular disease. High cholesterol has also been linked to diabetes and high blood pressure. To prevent or manage these conditions, work with your doctor to see what steps you need to take to lower your cholesterol.

The main risk from high cholesterol is coronary heart disease if the cholesterol level is too high, Cholesterol can build up in the walls of your arteries. Over time, this buildup called plaque) causes hardening of the arteries or atherosclerosis. This causes arteries to become narrowed, which slows the blood flow to the heart muscle. Reduced blood flow can result in angina (chest pain) or in a heart attack if a blood vessel gets blocked completely

CHOLESTEROL AND STROKE

Atherosclerosis causes arteries that lead to the brain to become

narrowed and even blocked.

If a vessel carrying blood to the brain is blocked completely, you

could have a stroke.

CHOLESTEROL AND PERIPHERAL VASCULAR DISEASE

High cholesterol also has been linked to peripheral vascular disease.

This refers to diseases of blood vessels outside the heart and brain.

In this condition, fatty deposits build up along artery walls and affect

blood circulation. This occurs mainly in arteries that lead to the legs

and feet.

CHOLESTEROL AND DIABETES Diabetes can upset the balance between HDL and LDL cholesterol levels. People with diabetes tend to have LDL particles that stick to arteries and damage blood vessel walls more easily. Glucose (a type of sugar) attaches to lipoproteins (a cholesterol-protein package that enables cholesterol to travel through blood). Sugarcoated LDL remains in the bloodstream longer and may lead to the formation of plaque. People with diabetes tend to have low HDL and high triglyceride (another kind of blood fat) levels. Both of these boost the risk of heart and artery disease.

CHOLESTEROL AND HIGH BLOOD PRESSURE

High blood pressure (also called hypertension) and high cholesterol

also are linked.

When the arteries become hardened and narrowed with cholesterol

plaque and calcium, the heart has to strain much harder to pump

blood through them.

As a result, blood pressure becomes abnormally high. High blood

pressure is also linked to heart disease.

Everyone older than age 20 should get their cholesterol levels

measured at least once every five years.

High cholesterol does not cause symptoms; so many people are

unaware that their cholesterol levels are too high.

Lowering cholesterol levels that are too high lessens the risk for

developing heart disease and reduces the chance of a heart attack or

dying of heart disease, even if you already have it.

To assess your cholesterol level, your doctor will usually ask for a

simple blood test called a lipoprotein profile. The lipoprotein profile

evaluates the following:

HDL (high density lipoprotein cholesterol, also called "good"

cholesterol)

LDL (low density lipoprotein cholesterol, also called "bad"

cholesterol)

Total cholesterol level

Triglycerides

In addition to the blood test, your doctor will perform a full physical

exam, discussing your medical history, checking your heart rate,

listening to your heartbeat, and taking your blood pressure.

If your cholesterol is found to be high, especially if you have other

risk factors for heart disease, your doctor will recommend various

treatment options ranging from dietary and lifestyle changes to

medication to lower your cholesterol.

LDL Cholesterol

LDL cholesterol can build up on the walls of your arteries and

increase your chances of getting heart disease. That is why LDL

cholesterol is referred to as "bad" cholesterol. The lower your LDL

cholesterol number, the lower your risk.

If your LDL is 190 or more, it is considered very high. Your doctor

will most likely recommend a statin in addition to making healthy

lifestyle choices. Statins are medicines that can help lower

cholesterol levels.

You may also need to take a statin even though your LDL level is

lower than 190. After figuring your 10-year risk, your doctor will

recommend a percentage by which you should try to lower your

LDL level through diet, exercise, and medication if necessary.

HDL Cholesterol

When it comes to HDL cholesterol -- "good" cholesterol – a higher

number means lower risk. This is because HDL cholesterol protects

against heart disease by taking the "bad" cholesterol out of your

blood and keeping it from building up in your arteries. A statin can

slightly increase your HDL, as can exercise.

Triglycerides

Triglycerides are the form in which

most fat exists in food and the body.

A high triglyceride level has been

linked to higher risk of coronary

artery disease. Here's the breakdown.

Triglycerides Triglyceride

Category

Less than 150 Normal

150 - 199 Mildly High

200 - 499 High

500 or higher Very high

Total Cholesterol

Your total blood cholesterol is a measure of LDL cholesterol, HDL

cholesterol, and other lipid components.

Your doctor will use your total cholesterol number when

determining your risk for heart disease and how best to manage it.

Doctors emphasize diet, exercise, and weight loss to reduce

cholesterol. Medications are another important option to lower heart

disease risk.

If you have high blood pressure, high cholesterol, or a history of

heart problems, you have a higher risk of heart attack and stroke.

You can lower your risk by making this small change: At each meal,

choose foods that are good for your heart.

Most diets are based on foods you shouldn’t eat. Instead, take a

positive approach and focus on foods that are good for you.

Eat more beans, legumes (like lentils), seeds, and nuts. Your weekly target: 4 servings of either nuts, seeds, or legumes such as black beans, garbanzos (also called chickpeas), or lentils.

Eat more vegetables, fruits, and whole grains. The fiber in these foods helps lower “bad” LDL cholesterol. Put these on your plate with every meal to reach these daily amounts: At least 5 cups of fruits and vegetables and three 1-ounce servings of whole grains a day.

Celebrate each pound you lose. Small steps add up. Dropping even 5 or 10 pounds -- even if you're still technically overweight afterward -- will cut your risk of having a heart attack or stroke by lowering your blood pressure, cholesterol, and blood sugar levels.

Feed your body regularly. When you skip a meal, you’re more likely to overeat later. For some people, eating 5 to 6 mini-meals works best to limit calories, help control blood sugars, and regulate metabolism. For others, 3 meals a day works better, since extra meals can trigger overeating. See which approach works for you.

Eating sterol and stanol-containing foods is an easy way to

lower your LDL cholesterol, which helps reduce the risk of

heart disease

The New Low-Cholesterol Diet: Plant Sterols and Stanols

Plant sterols and stanols are substances that occur naturally in

small amounts in many grains, vegetables, fruits, legumes, nuts,

and seeds. Since they have powerful cholesterol-lowering

properties, manufacturers have started adding them to foods.

You can now get stanols or sterols in margarine spreads,

orange juice, cereals, and even granola bars.

On a molecular level, sterols and

stanols look a lot like cholesterol.

So when they travel through

your digestive tract, they get in the

way.

They can prevent real cholesterol

from being absorbed into your

bloodstream.

Instead of clogging up your

arteries, the cholesterol just goes

out with the waste.

Plant stanol esters help block the absorption of cholesterol.

Research shows that three servings a day can reduce cholesterol by

20 points.

Experts have been studying the effects of food fortified with plant

sterols for decades.

One important study of people with high cholesterol found that less

than an ounce of stanol-fortified margarine a day could lower "bad"

LDL cholesterol by 14%.

The results were published in The New England Journal of Medicine.

You can also find plant sterols or stanols in some cooking oils, salad dressings, milk, yogurt, snack bars, and juices. Indeed, so many fortified products are headed to grocery store shelves that you'll soon have a dizzy array of choices. But check the label carefully. While plant sterols are healthy, extra calories are not. Excess calories simply lead to excess pounds.

Nuts get a bad rap because of fat and calories. But they're

a great weapon against LDL, the bad cholesterol.

The New Low-Cholesterol Diet: Nuts

Nuts get a bad rap. A lot of people still see them as salty,

fatty, and high calorie but also have lots of protein, fiber,

healthy monounsaturated fats, vitamins, nutrients, and

antioxidants. And many studies have shown that nuts have

powerful cholesterol-lowering effects.

The Nuts

Basically, nuts are good,

They're high in vitamins, minerals,

and good monounsaturated fat,

which can lower cholesterol.

Along with almonds and walnuts,

the FDA gave its qualified health

claim to peanuts, hazelnuts, pecans, some pine nuts, and

pistachios.

How Much Do You Need?

You can get the health benefits of nuts from just a

handful a day. About 1 to 1.5 ounces is plenty,

experts say. The high protein and fiber in nuts make

them very filling. Make sure you don't overdo it.

Improve total cholesterol with omega-3 fatty acids found

in salmon, tuna, sardines, and more.

The term "fatty fish" may sound unappealing, but actually these are

the tastiest and healthiest foods from the sea. Oily fish such as

salmon, tuna, sardines, mackerel, and trout are full of omega-3 fatty

acids -- good fats unlike the bad saturated fat you find in most meats.

These fish should be a staple of everyone's heart-healthy diet.

Omega-3 fatty acids have been shown to lower triglycerides, which

are a type of fat in the bloodstream. Experts aren't sure of the exact

mechanism. Omega-3 fatty acids may also slow down the growth of

plaques in the arteries and reduce inflammation throughout the

body.

Getting daily omega-3 fatty acids from fish oil could lower triglyceride

levels by 25%-30%. The results were published in The American Journal

of Clinical Nutrition in 1997.

Fatty fish typically are cold-water fish. You have many good choices when

it comes to fatty fish. The American Dietetic Association recommends:

Salmon, Tuna

Trout, Herring, Sardines, Mackerel

Three ounces of salmon alone offers about 1 gram of EPA and DHA. If

these fish aren't to your taste, you can also try white fish such as halibut

or trout. A 3.5-ounce serving of trout offers about 1 gram of EPA, plus

DHA.

EPA and DHA stand for eicosapentaenoic acid

and docosahexaenoic acid respectively. These fatty

acids are omega-3 fats, which are found in cold water

fish.

EPA DHA are highly unsaturated fats because they

contain six and five double bonds on their long

structural chains. These polyunsaturated fats play a

very important role with the function of our bodies.

It can really bring down your bad LDL cholesterol levels without

lowering your good cholesterol. The same goes for oat bran, which is

in some cereals, baked goods, and other products.

How Do Oats Help?

Oatmeal is full of soluble fiber, which we know lowers LDL levels.

Experts aren't exactly sure how, but they have some ideas. When you

digest fiber, it becomes gooey. Researchers think that when it's in

your intestines, it sticks to cholesterol and stops it from being

absorbed. So instead of getting that cholesterol into your system --

and your arteries -- you simply get rid of it as waste.

Hypercholesterolemia medications

go in many types:

Statins (HMG CoA Reductase

Inhibitors)

Fibrates

Niacin

Cholesterol absorption inhibitors

Bile acid sequestrants

Omega-3 fatty acids, which we

talked about in previous slides.

Mechanism of action:

HMG CoA reductase inhibitors competitively inhibit the activity of HMG CoA reductase, the rate-limiting enzyme in cholesterol synthesis.

Inhibition of this enzyme results in a transient, modest decrease in cellular cholesterol concentration .

The decrease in cholesterol concentration activates a cellular signaling cascade culminating in the activation of sterol regulatory element binding protein (SREBP), a transcription factor that up-regulates expression of the gene encoding the LDL receptor.

Increased LDL receptor expression causes increased uptake of plasma LDL, and consequently decreases plasma LDL-cholesterol concentration. Approximately 70% of LDL receptors are expressed by hepatocytes, with the remainder expressed by a variety of cell types in the body.

CLINICAL USES

Hypercholesterolemia

Familial Hypercholesterolemia (Atorvastatin might be an exception)

Coronary atherosclerosis

Prophylaxis for coronary atherosclerosis.

ADVERSE EFFECTS AND CONTRAINDICATIONS

HMG-CoA inhibitors are contraindicated in pregnancy. Limited evidence from animal and human studies indicates that statins should not be taken during pregnancy.

Liver disfunction: Elevations of serum aminotransferase activity (up to three times normal) occur in some patients. This is often intermittent and usually not associated with other evidence of hepatic toxicity. In some patients, who may have underlying liver disease or a history of alcohol abuse, levels may exceed three times normal. This finding portends more severe hepatic toxicity.

A relatively common side effect of the statins

(perhaps 1% of patients) is myositis, thatis,

inflammation of skeletal muscle accompanied by

pain, weakness, and high levels of serum keratine

kinase.

Rhabdomyolysis, i.e., disintegration of muscle with

urinary excretion of myoglobin and kidney damage,

is serious side effect.

Crestor :

WHAT IS CRESTOR?

Crestor is in a group of drugs called HMG CoA reductase inhibitors, or "statins."

Rosuvastatin reduces levels of "bad" cholesterol (low-density lipoprotein, or LDL) and triglycerides in the blood, while increasing levels of "good" cholesterol (high-density lipoprotein, or HDL).

Crestor is used to lower cholesterol and triglycerides (types of fat) in the blood.

Crestor is also used to lower the risk of stroke, heart attack, and other

heart complications in people with diabetes, coronary heart disease,

or other risk factors.

Crestor is used in adults and children who are at least 10 years old.

IMPORTANT INFORMATION

You should not take Crestor if you are allergic to rosuvastatin, if you

are pregnant or breast-feeding, or if you have liver disease. Stop

taking this medication and tell your doctor right away if you become

pregnant.

Before taking Crestor, tell your doctor if you have ever had liver or

kidney disease, diabetes, or a thyroid disorder, if you are of Chinese

descent, or if you drink more than 2 alcoholic beverages daily.

BEFORE TAKING THIS MEDICINE

You should not take Crestor if you are allergic to rosuvastatin, if you are pregnant or breast-feeding, or if you have liver disease.

To make sure you can safely take Crestor, tell your doctor if you have any of these other conditions:

history of liver disease

history of kidney disease

diabetes;

a thyroid disorder

CRESTOR SIDE EFFECTS

Rare

Dark-colored urine fever

muscle cramps or spasms

muscle pain, stiffness, tenderness, wasting, or weakness

unusual tiredness or weakness

GENERAL DOSING INFORMATION The dose range for CRESTOR is 5 to 40 mg orally once daily. The usual

starting dose is 10-20 mg.

CRESTOR can be administered as a single dose at any time of day, with or

without food.

When initiating CRESTOR therapy or switching from another HMG-CoA

reductase inhibitor therapy, the appropriate CRESTOR starting dose

should first be utilized, and only then titrated according to the patient’s

response and individualized goal of therapy.

After initiation or upon titration of CRESTOR, lipid levels should be

analyzed within 2 to 4 weeks and the dosage adjusted accordingly.

Rosuvastatin

Heterozygous Familial Hypercholesterolemia in Pediatric Patients (10 to 17 years of age)

The usual dose range of CRESTOR is 5-20 mg/day; the maximum recommended dose is 20 mg/day (doses greater than 20 mg have not been studied in this patient population).

Homozygous Familial Hypercholesterolemia

The recommended starting dose of CRESTOR is 20 mg once daily. Response to therapy should be estimated from preapheresis LDL-C levels.

Dosing in Asian Patients

In Asian patients, consider initiation of CRESTOR therapy

with 5 mg once daily due to increased rosuvastatin

plasma concentrations. The increased systemic exposure

should be taken into consideration when treating Asian

patients not adequately controlled at doses up to

20 mg/day .

Figure: Label of Crestor (20mg tablets). Produced by AstraZeneca™

WHAT IS ZOCOR?

Zocor belongs to a group of drugs called HMG CoA reductase

inhibitors, or "statins." Simvastatin reduces levels of "bad"

cholesterol (low-density lipoprotein, or LDL) and triglycerides in the

blood, while increasing levels of "good" cholesterol (high-density

lipoprotein, or HDL) .

Zocor is used to lower cholesterol and triglycerides (types of fat) in

the It is also used to lower the risk of stroke, heart attack, and other

heart complications in people with diabetes, coronary heart disease,

or other risk factors.

Zocor is used in adults and children who are at least 10 years old.

IMPORTANT INFORMATION

In rare cases, Zocor can cause a condition that results in the breakdown of skeletal muscle tissue, leading to kidney failure.

Never take Zocor in larger amounts, or for longer than recommended by your doctor.

Taking too much of this medication may cause serious or life-threatening side effects.

Before taking Zocor, tell your doctor if you have ever had liver or kidney disease, diabetes, or a thyroid disorder, if you are of Chinese descent, or if you drink more than 2 alcoholic beverages daily.

Zocor can harm an unborn baby or cause birth defects. Do not use if you are pregnant.

ZOCOR SIDE EFFECTS

If any of the following side effects occur while taking simvastatin,

check with your doctor immediately:

More common

Dizziness

fainting

fast or irregular heartbeat

Generic name: simvastatin

Dosage form: tablet, film coated

The usual dosage range is 5 to 40 mg/day.

The recommended usual starting dose is 10 or 20 mg once a day in the evening.

In patients with CHD or at high risk of CHD, ZOCOR can be started simultaneously with diet.

For patients at high risk for a CHD event due to existing CHD, diabetes, peripheral vessel disease, history of stroke or other cerebrovascular disease, the recommended starting dose is 40 mg/day.

Lipid determinations should be performed after 4 weeks of therapy and periodically thereafter.

Simvastatin

Figure: Label of Zocor (10mg tablets). Produced by MERCK & CO. INC™

Zetia reduces the amount of cholesterol or other sterols that your body absorbs from your diet.

Zetia is used to treat high cholesterol, along with a low-fat, low-cholesterol diet. It is sometimes given with other cholesterol-lowering medications. It is also used to treat high blood sitosterol and campesterol along with diet therapy.

IMPORTANT INFORMATION

Zetia is only part of a complete program of treatment that also includes diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely.

Some cholesterol medications should not be taken at the same time. Do not take Zetia with cholestyramine (Prevalite, Questran), colestipol (Colestid), or colesevelam (Welchol). Wait at least 4 hours after taking any of these medicines before you take Zetia. You may also take Zetia 2 hours before taking any of these other medicines.

Zetia may be taken at the same time with fenofibrate (Antara, Lipofen, Lofibra, TriCor, Triglide), or with any of the "statin" drugs such as lovastatin (Mevacor), simvastatin (Zocor), pravastatin (Pravachol), fluvastatin (Lescol), atorvastatin (Lipitor), or cerivastatin (Baycol).

In rare cases, cholesterol-lowering medication can cause a condition that results in the breakdown of skeletal muscle tissue. This condition can lead to kidney failure. Call your doctor at once if you have unexplained muscle pain or tenderness, muscle weakness, fever or flu symptoms, and dark colored urine.

ZETIA SIDE EFFECTS

Some ezetimibe side effects may not need any medical attention. As your body gets used to the medicine these side effects may disappear. Your health care professional may be able to help you prevent or reduce these side effects, but do check with them if any of the following side effects continue, or if you are concerned about them:

More common

Fever

headache

muscle pain

runny nose

sore throat

Less common

Back pain

Body aches or pain

Chest pain

Chills

Active ingredient: ezetimibe Dosage form: tablet

General Dosing Information

The recommended dose of ZETIA is 10 mg once daily. ZETIA can be administered with or without food.

Concomitant Lipid-Lowering Therapy

ZETIA may be administered with a statin (in patients with primary hyperlipidemia) or with fenofibrate (in patients with mixed hyperlipidemia) for incremental effect. For convenience, the daily dose of ZETIA may be taken at the same time as the statin or fenofibrate, according to the dosing recommendations for the respective medications.

Co-administration with Bile Acid Sequestrants

Dosing of ZETIA should occur either ≥2 hours before or ≥4 hours after administration of a bile acid sequestrant.

Ezetimibe

Patients with Hepatic Impairment

No dosage adjustment is necessary in patients with mild hepatic impairment.

Patients with Renal Impairment

No dosage adjustment is necessary in patients with renal impairment. When given with simvastatin in patients with moderate to severe renal impairment (estimated glomerular filtration rate <60 mL/min/1.73 m2), doses of simvastatin exceeding 20 mg should be used with caution and close monitoring.

Geriatric Patients

No dosage adjustment is necessary in geriatric patients.

Figure: Label of Zetia (10mg tablets). Produced by Schering Corporation™

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