Drug Therapy for Cholesterol

What drugs are most commonly used to treat high cholesterol?

The drugs of first choice for elevated LDL cholesterol are the HMG CoA
reductase inhibitors, e.g., atorvastatin, fluvastatin, lovastatin,pravastatin,
rosuvastatin and simvastatin. Statin drugs are very effective for lowering
LDL cholesterol levels and have few immediate short-term side effects.

• They are easy to administer, have high patient acceptance and have few
drug-drug interactions.
• Patients who are pregnant, have active or chronic liver disease, or who
are allergic to statins shouldn't use statin drugs.
• The most common side effects are gastrointestinal, including constipation
and abdominal pain and cramps. These symptoms are usually mild to
severe and generally subside as therapy continues.

Another class of drugs for lowering LDL is the bile acid sequestrants —
colesevelam, cholestyramine and colestipol — and nicotinic acid(niacin).
These have been shown to reduce the risk for coronary heart disease in
controlled clinical trials. Both classes of drugs appear to be free of serious side
effects. But both can have troublesome side effects and require considerable
patient education to achieve adherence.Nicotinic acid is preferred in patients
with triglyceride levels that exceed 250 mg/dL because bile acid
sequestrants tend to raise triglyceride levels.

Niacin (nicotinic acid) comes in prescription form and as “dietary supplements.”

Dietary supplement niacin is not regulated by the U.S. Food and Drug
Administration (FDA) the same way that prescription niacin is. It may contain
widely variable amounts of niacin — from none to much more than the label
states. The amount of niacin may even vary from lot to lot of the same brand.

• Dietary supplement niacin must not be used as a substitute for

prescription niacin. It should not be used for cholesterol lowering because
of potentially very serious side effects.

What other drugs are available to treat high cholesterol?

Other available drugs are gemfibrozil, fenofibrate and clofibrate. These fibric
acid derivatives are primarily used for lowering high triglyceride levels.

If a patient doesn't respond adequately to single drug therapy, combined drug

therapy should be considered to further lower LDL cholesterol levels. For patients
with severe hypercholesterolemia, combining a bile acid sequestrant with either
nicotinic acid or lovastatin has the potential to markedly lower LDL cholesterol.
For hypercholesterolemic patients with elevated triglycerides, nicotinic acid or
gemfibrozil should be considered as one agent for combined therapy.

How Do Cholesterol Lowering Drugs Affect

Cholesterol
Cholesterol lowering drugs are often used as a last resort when it
comes to your lipid lowering therapy - often after lifestyle
modifications, such as smoking cessation, low fat diet, and exercise do
not work to effectively manage your cholesterol.

Typically, eating healthy and exercising regularly are the two most
essential ingredients needed to keep cholesterol levels within normal
range. Sometimes, however, this may not work, and your health-care
provider may want to place you on medication. Many cholesterol-
lowering medications are currently on the market, and each of these
medications lower cholesterol levels in different ways. Additionally,
each of these drugs target different aspects of your lipid profile. For
instance, some drugs may only be effective in lowering your LDL
(“bad” cholesterol) levels, where as other drugs may target every
aspect of your lipid profile. In any case, your health-care provider will
weigh the benefits and risks of each drug, and select the best
cholesterol-lowering medication for you.

Statins
Statins, also known as HMG-CoA reductase inhibitors, are the most
commonly prescribed cholesterol-lowering medications. Although they
have received a bad reputation for some of the undesirable, but
rare, side effects, they target every aspect of your cholesterol profile.
They decrease LDL between 18 and 65 percent, increase HDL (the
“good” cholesterol) up to 5 to 15 percent, and
decrease triglycerides by 7 to 30 percent. Not only are statins effective
in normalizing all aspects of your cholesterol profile, they have been
also noted to possess anti-inflammatory properties that are being
further investigated in areas such as heart disease and some types
of cancer. They also stabilize plaques that have already formed, thus
preventing them from rupturing and causing a subsequent stroke.
Statins also reduce the likelihood of developing blood clots, improve
vascular function, reduce cardiac arrhythmias, and may cause plaque
reduction. With these extra benefits of statins, these drugs are the
most widely prescribed of the cholesterol-lowering medications. Some
studies have shown a reduction in the incidence of death even in
patients with normal cholesterol levels.
Commonly prescribed statins include the following:

• Atorvastatin (Lipitor®)

• Fluvastatin (Lescol®)

• Lovastatin (Mevacol®)

• Pitavastatin (Livalo®; approved in August 2009)

• Pravastatin (Pravachol®)

• Rosuvastatin calcium (Crestor®)

• Simvastatin (Zocor®)

Rare side effects associated with statins include mild inflammation of the liver,

muscle inflammation, pain, and weakness. Inflammation of the liver can be

detected by liver function tests, which usually are performed once or twice during

the first several months of therapy and periodically (e.g., twice a year) thereafter.

Patients who experience severe muscle pain or weakness or any uncomfortable

side effect should speak with their physician.

Lipitor® has been combined with the blood pressure-lowering drug

Norvasc® to treat patients with high cholesterol and high blood pressure.

This combination drug, which is called Caduet®, offers the convenience of

taking only one medication to control both conditions.

Bile Acid Resins

Bile acid resins reduce cholesterol absorption from the small intestine
to the bloodstream. They typically work on LDL and HDL cholesterols,
although they are not as effective as statins. Bile acid resins reduce
LDL by 15 to 30 percent and raise HDL by 3 to 5 percent. Typically,
triglycerides are not touched by bile acid resins. In some cases, they
may actually raise triglycerides levels. These drugs commonly cause a
lot of bloating, nausea and cramping which greatly limits their use.
Additionally, some vitamins and drugs cannot be taken around the
time you take bile acid resins, since their absorption is limited and may
make them ineffective.
Nicotinic Acid
Nicotinic acid, also known as vitamin B3 or niacin, also works on all
aspects of your lipid profile. However, it is most notable for raising HDL
levels (up to 15 to 35 percent) and lowering triglyceride levels (by
between 20 and 50 percent). It also lowers LDL, but not as much as
statins. Niacin lowers LDL levels on an average between 5 to 25
percent. Flushing occurs in about 50 percent of individuals who take
this drug. This symptom can be intolerable and is the most common
reason why this drug is discontinued. With the exception of Niaspan®
(a sustained release niacin preparation only available by prescription),
sustained release niacin products tend to produce liver toxicity
compared to immediate-release niacin. Additionally, the “no-flush”
niacin products available over the counter are not regulated by the
Food and Drug Administration and may not contain the free nicotinic
acid needed to lower cholesterol. So these drugs may be ineffective.
Fibric Acids
Fibric acids, or fibrates, are most noted for their ability to
lower triglycerides, which can be lowered on an average of 20 to 50
percent. They also lower LDL levels by between 5 to 20 percent and
raise HDL levels by 10 to 20 percent. This class of drugs has been
known to produce muscle toxicity, especially when combined with
other drugs such as statins and warfarin (Coumadin®). In this case,
your physician may either adjust the dose of your drug (as in the case
of warfarin) or avoid the combination altogether (in the case of
statins).
Absorption Inhibitors
Ezetimibe is currently the only drug in this class and primarily targets
LDL cholesterol levels, lowering LDL levels by an average of 15
percent. Typically, ezetimibe is coupled with a statin to ensure a
powerful effect when lowering LDL levels. Triglycerides are usually not
effected by ezetimibe, while HDL levels are only slightly raised (by
about 5 percent). Liver and muscle problems have been reported with
ezetimibe; however, the incidence of this occurrence is low.

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http://cholesterol.about.com/od/treatments/CholesterolLowering_Medications_and_Treatments.htm
Statin Drugs (http://cholesterol.about.com/od/statindrugs/Statin_Drugs.htm)
Statins are the most commonly prescribed family of medications used
to treat high cholesterol that cannot be controlled with diet and
exercise alone.
13. Atorvastatin (Lipitor) (5)
14. Fluvastatin (Lescol) (5)
15. Livalo (1)
16. Lovastatin (7)
9. Pravastatin (5)
10. Rosuvastatin (Crestor) (6)
11. Simvastatin (Zocor) (5)

What Are Statins?

Statin drugs, also known as HMG CoA reductase inhibitors, are a
popular class of cholesterol-lowering drugs that also have other
healthy benefits.
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How Do I Take My Statin?

Statins are a popular class of cholesterol lowering drugs that lower
LDL, raise HDL, and lower triglycerides. Like other drugs, in order for
them to work properly, you need to know how to take them. When
taken correctly, statins may lower your cholesterol and cut your risk for
heart disease.

What Should I Tell My Health Care Provider Before Starting

Statin Therapy?
Statins lower ldl cholesterol and lower triglycerides. Statins also raise
hdl cholesterol. There are some conditions that may prevent you from
taking a statin. Additionally, statin drug interactions may occur.

When Is The Best Time To Take My Statin?

Statins are a popular cholesterol lowering drug. The majority of
cholesterol is made during the night. Therefore, dosing statins at night
would be best to get the most cholesterol lowering effect.

Muscle Pain and Statins

Statins are cholesterol-lowering medications that lower ldl cholesterol
and raise hdl cholesterol. One of the most important statin side effects
is muscle pain. Scientists may have discovered the gene that causes
muscle pain caused by statins.
Can Coenzyme Q10 Reduce Muscle Pain Associated With
Statins?
Statins, a class of the most popular cholesterol-lowering drug, raise
HDL and lower LDL and triglycerides. But statins may also cause
muscle pain and weakness. Some believe that coenzyme Q10, which is
depleted by statins, is responsible for the muscle pain and weakness
associated with statin use. Will CoQ10 supplements help?

Are Statin Side Effects Worth The Price In The Fight Against
Heart Disease?
Statins are the most commonly prescribed cholesterol lowering
medications. Statins lower ldl and triglycerides and raise hdl levels.
The two most common side effects associated with taking statins are
muscle pain and weakness and liver problems.

Could Your Statin Be Causing You To Lose Sleep?

Statins are very effective in lowering cholesterol. This cholesterol
lowering medication lowers ldl, raise hdl, and lowers triglycerides.
Statins are also associated with some side effects. One of the lesser
known side effects of statin is sleep disturbances.

Should I Drink Grapefruit Juice With My Statin?

Statins help keep high cholesterol in check. If you take a statin, you
should strictly watch your intake of grapfruit juice.
Do Statins Have Other Effects - Besides Lowering Cholesterol?
Statins are most famous for lower cholesterol levels, but studies are
suggesting that statins have other healthy benefits, too. Scientists
contribute this to the anti-inflammatory properties that statins possess.
Find out what other possible benefits that statins may have.
Before You Buy Statins
Dr. Richard Fogoros, About.com's Guide to Heart Disease, has devised
a comprehensive review of statins, including why they are so unique,
which ones are the cheapest, and who actually benefits from taking
them.

Statins May Modestly Reduce Blood Pressure

Statins lower cholesterol, but have a variety of other benefits, too,
such as preventing heart disease and plaque formation. A new study
has found that statins may also lower blood pressure.

Statins May Improve Lung Function

Statins are a cholesterol lowering medication known for lowering ldl,
raising hdl, and lowering triglycerides. Additionally, statins are known
for preventing heart attacks and strokes in individuals with heart
disease. A recent paper suggests that statins may increase lung
function. The ability of statins to increase lung function may be due to
preventing inflammation.

Could A Statin A Day Keep Alzheimer's Disease At Bay?

Statin drugs are commonly prescribed cholesterol-lowering
medications that are also used to reduce inflammation and the risk of
heart disease. Now, it has been found that statins may reduce the risk
of Alzheimer's disease.

Older Patients May Benefit From High-Dose Statin Therapy

A study published in the Annals of Internal Medicine states that high-
dose atorvastatin (Lipitor) may reduce the incidence of cardiovascular
events in patients who already have heart disease. Additionally, this
high-dose statin therapy lowers LDL cholesterol greatly.

Statin Drugs May Help in Treating Hepatitis C

Masanori Ikeda and colleagues of Okayama University in Japan have
found a new use for cholesterol-lowering statin drugs. The researchers
discovered the possibility that statins may help treat patients with
hepatitis C infections. This study was published in Hepatology, a
journal published by the American Association for the Study of Liver
Disease, this month.

Taking Statin Drugs May Lower Your Risk of Cancer

New evidence suggests that statin drugs may lower your risk of certain
cancers. The data, which was released by two research groups at a
conference yesterday, gave preliminary evidence that individuals
taking statin drugs may lower their incidence of getting certain
cancers.

Can Statins Lower Your Cancer Risk?

Statins may have a few undesirable side effects, but they also have
some beneficial properties, too. In fact, there has been a lot of
research investigating the treatment of certain cancers with statins.

Using Statins In Kids: Are They Safe?

Although high cholesterol is fairly rare in children, it can happen -
especially if it runs in the family. In some cases, children may need to
turn to cholesterol-lowering drugs - including statins - to help lower
their cholesterol levels. But are they safe to use in this younger
population?

Statins And Inflammation

While statins possess cholesterol-lowering properties, they have
additional added benefits, too. Statins have anti-inflammatory
properties that can prevent you from suffering from a heart attack or
stroke.

Can I Take a Statin if I Am Pregnant or Planning to Become

Pregnant?
If you are planning to become pregnant or just found out you're
pregnant, you should not take a statin.

Can You Take Statins and Fibrates Together?

Although statins and fibrates can potentially interact with one another,
this combination is commonly used to optimally treat high cholesterol
and triglyceride levels.

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A Comparison of Simvastatin and Atorvastatin up to Maximal

Recommended Doses in a Large Multicenter Randomized
Clinical Trial

http://www.medscape.com/viewarticle/407812

Simvastatin, across a range of doses, will be more effective than atorvastatin at

raising HDL cholesterol and apo A-I levels.