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 i
nhibitors, e.g.,€atorvastatin,€fluvastatin, lovastatin,pravastatin, rosuvastatin€and s
imvastatin. 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-dr
ug interactions.
* Patients who are pregnant, have active or chronic liver disease, or who are al
lergic 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 general
ly subside as therapy continues.
Another class of drugs for lowering LDL is the€bile acid sequestrants€ colesevelam,€chol
estyramine€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 d
rugs appear to be free of serious side effects. But both can have troublesome si
de effects and require considerable patient education to achieve adherence.Nicot
inic acid is preferred in patients with triglyceride levels that exceed 250 mg/d
L because bile acid sequestrants tend to raise triglyceride levels.
Niacin€(nicotinic acid) comes in prescription form and as dietary supplements. Dieta
ry 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 am
ounts of niacin€ €from€none€to much more than the label states. The amount of niacin may e
ven 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 s
ide effects.
What other drugs are available to treat high cholesterol?
Other available drugs are€gemfibrozil,€fenofibrate€and€clofibrate. These fibric acid der
ivatives are primarily used for lowering high triglyceride levels.
If a patient doesn't respond adequately to single drug therapy, combined drug th
erapy 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 cholestero
l. 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 c
essation, low fat diet, and exercise do not work to effectively manage your chol
esterol.
Typically, eating healthy and exercising regularly are the two most essential in
gredients needed to keep cholesterol levels within normal range. Sometimes, howe
ver, this may not work, and your health-care provider may want to place you on m
edication. Many cholesterol-lowering medications are currently on the market, an
d each of these medications lower cholesterol levels in different ways. Addition
ally, each of these drugs target different aspects of your lipid profile. For in
stance, some drugs may only be effective in lowering your LDL ( bad cholesterol) le
vels, 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 presc
ribed cholesterol-lowering medications. Although they have received a bad reputa
tion 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€HD
L€(the good cholesterol) up to 5 to 15 percent, and decrease€triglycerides€by 7 to 30 pe
rcent. Not only are statins effective in normalizing all aspects of your cholest
erol 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€c
ancer. They also stabilize plaques that have already formed, thus preventing the
m from rupturing and causing a subsequent stroke. Statins also reduce the likeli
hood of developing blood clots, improve vascular function, reduce cardiac arrhyt
hmias, and may cause plaque reduction. With these extra benefits of statins, the
se 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, mu
scle inflammation, pain, and weakness. Inflammation of the liver can be detected
by liver function tests, which usually are performed once or twice during the f
irst several months of therapy and periodically (e.g., twice a year) thereafter.
Patients who experience severe muscle pain or weakness or any uncomfortable sid
e effect should speak with their physician.
Lipitor® has been combined with the blood pressure-lowering drug Norvasc® to treat p
atients with high cholesterol and high blood pressure. This combination drug, wh
ich is called Caduet®, offers the convenience of taking only one medication to con
trol both conditions.

Bile Acid Resins

Bile acid resins reduce cholesterol absorption from the small intestine to the b
loodstream. They typically work on LDL and HDL cholesterols, although they are n
ot 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 ac
id resins. In some cases, they may actually raise triglycerides levels. These dr
ugs commonly cause a lot of bloating, nausea and cramping which greatly limits t
heir 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 i
neffective.
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 1
5 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 individ
uals 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 ni
acin products tend to produce liver toxicity compared to immediate-release niaci
n. Additionally, the no-flush niacin products available over the counter are not r
egulated by the Food and Drug Administration and may not contain the free nicoti
nic 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 triglycerid
es, 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 combi
ned 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) o
r avoid the combination altogether (in the case of statins).
Absorption Inhibitors
Ezetimibe is currently the only drug in this class and primarily targets LDL cho
lesterol levels, lowering LDL levels by an average of 15 percent. Typically, eze
timibe is coupled with a statin to ensure a powerful effect when lowering LDL le
vels. Triglycerides are usually not effected by ezetimibe, while HDL levels are
only slightly raised (by about 5 percent). Liver and muscle problems have been r
eported with ezetimibe; however, the incidence of this occurrence is low.
========================================= http://cholesterol.about.com/od/treatm
ents/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 hig
h 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)
Other cholesterol-lowering medications€can be used alone, or combined with a stati
n, to reduce cholesterol to an acceptable level. Combining medications mayincrea
se the risk€for liver and/or muscle inflammation.
Other medications include the following:
* Cholestyramine (LoCHOLEST®, Questran®)
* Colestipol (Colestid®)
* Fenofibrate (Tricor®)
* Fluvastatin (Lescol®)
* Gemfibrozzil (Lopid®)
* Niacin (Niacinol®, Niacor®, Nicolar®, Slo-Niacin®)

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 proper
ly, you need to know how to take them. When taken correctly, statins may lower y
our 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 ch
olesterol. 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 t
he most cholesterol lowering effect.
Muscle Pain and Statins
Statins are cholesterol-lowering medications that lower ldl cholesterol and rais
e 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 stati
ns.
Can Coenzyme Q10 Reduce Muscle Pain Associated With Statins?
Statins, a class of the most popular cholesterol-lowering drug, raise HDL and lo
wer 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. Stati
ns lower ldl and triglycerides and raise hdl levels. The two most common side ef
fects associated with taking statins are muscle pain and weakness and liver prob
lems.
Could Your Statin Be Causing You To Lose Sleep?
Statins are very effective in lowering cholesterol. This cholesterol lowering me
dication lowers ldl, raise hdl, and lowers triglycerides. Statins are also assoc
iated 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 st
rictly 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 th
e anti-inflammatory properties that statins possess. Find out what other possibl
e benefits that statins may have.
Before You Buy Statins
Dr. Richard Fogoros, About.com's Guide to Heart Disease, has devised a comprehen
sive review of statins, including why they are so unique, which ones are the che
apest, 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 pr
eventing 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 hd
l, and lowering triglycerides. Additionally, statins are known for preventing he
art attacks and strokes in individuals with heart disease. A recent paper sugges
ts that statins may increase lung function. The ability of statins to increase l
ung 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 a
lso 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 atorv
astatin (Lipitor) may reduce the incidence of cardiovascular events in patients
who already have heart disease. Additionally, this high-dose statin therapy lowe
rs LDL cholesterol greatly.
Statin Drugs May Help in Treating Hepatitis C
Masanori Ikeda and colleagues of Okayama University in Japan have found a new us
e for cholesterol-lowering statin drugs. The researchers discovered the possibil
ity 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, g
ave preliminary evidence that individuals taking statin drugs may lower their in
cidence of getting certain cancers.
Can Statins Lower Your Cancer Risk?
Statins may have a few undesirable side effects, but they also have some benefic
ial 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 cholester
ol-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 adde
d 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 sh
ould not take a statin.
Can You Take Statins and Fibrates Together?
Although statins and fibrates can potentially interact with one another, this co
mbination 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 a
t raising HDL cholesterol and apo A-I levels.