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    Cholesterol Reducing DrugsCholesterol-reducing drugs are medications that lower the levels of fats ( lipids) in the blood, including cholesteroland triglycerides. High levels of these fats in the bloodstream increase the risk of Coronary artery disease,heart attack, stroke and other heart-related conditions. Therefore, cholesterol reducers and other antilipemicmedications are often prescribed for people with high cholesterol levels (hypercholesterolemia) or other elevated

    lipid levels (e.g., high triglycerides).

    There are five main categories of cholesterol reducers: statins, bile acid resins, nicotinic acid, fibrates andezetimibe. Most are available only by prescription, while nicotinic acid, a form of vitamin B3 (niacin), is availableover-the-counter. However, niacin should only be taken under the care of a physician to monitor any side effectsthat could arise, such as severe upset stomach (nausea) and flushing.

    Cholesterol-reducing drugs are medications that lower the levels of fats (lipids) in the blood, including cholesteroland triglycerides. Besides lowering total cholesterol and LDL (bad)cholesterol levels , some cholesterol-lowering medications may also modestly increase levels of HDL (good) cholesterol. High LDL cholesterol levelsand low HDL cholesterol levels are associated with heart attack, stroke and coronary artery disease.

    Cholesterol-reducing drugs work on lipids in the bloodstream. Some work by reducing the amount of cholesterolor triglycerides produced or absorbed in the body. Others remove cholesterol that has built up in the arteries. Themechanisms and strengths of each type of cholesterol-reducing drug varies.

    In general, cholesterol is a waxy type of fat that is produced naturally by the body and consumed in relativelymodest amounts through the diet. Cholesterol is important because it is used as a building block for hormones,such as estrogen and testosterone. Cholesterol itself is carried through the bloodstream in a package known as alipoprotein. Researchers have identified a number of different lipoproteins, each of which interacts with the bodyin a different way. High-density lipoproteins, or HDLs, are compact packages that can remove cholesterol fromarteries, thus reducing the risk ofheart attack and stroke. Other types of lipoproteins, including low-densitylipoproteins (LDL), very low-density lipoproteins (VLDL) and intermediate density lipoproteins, are unstablepackages that can deposit cholesterol into an artery, thus accelerating atherosclerosis and raising the risk ofheart attack and stroke. triglycerides are another type of fat that are associated with increased cardiovascularrisk.

    The point of cholesterol-lowering medications is tofavorably affect the lipid profile, or relative levels of HDLand LDL cholesterol in the bloodstream. Studies have

    shown that patients who have very high HDL levelsexperience a protective effect, while patients withelevated LDLs are at increased risk. Thus, cholesterol-lowering medications are routinely used to affect aperson's coronary risk profile. They may be prescribedby people who have already experienced a heart attackor stroke, who have undergone a catheter-basedtherapy such as angioplasty with or without stenting,bypass surgery, or even patients who are at risk ofdangerous arrhythmias.

    Different types of cholesterol reducers affect levels of fats (lipids) in different ways and generally fall into thefollowing categories:

    Statins. Considered the first line of treatment for most patients with high cholesterol(hypercholesterolemia), statins block the production of specific enzymes used by the body to makecholesterol. Statins have been shown to reduce the risk of a first heart attack, as well as recurrent heart

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    attacks in patients with known disease, and stroke. They have also been shown to reduce the risk ofdeath among patients with heart failure. Statins are particularly effective at lowering levels of LDL (bad)cholesterol and, to a lesser degree, triglycerides. While statins do increase levels of HDL (good)

    cholesterol, they do not seem to increase those levels as well as other cholesterol reducers do. Statinsgenerally have limited side effects, although there are some reports of a rare muscle deterioration calledrhabdomyolysis. Some media reports have also linked statins to reduced memory function, but thisappears to be a rare side effect. Periodic blood testing is advisable to monitor both the side effects on

    blood fats and to monitor liver function.

    The decision to administer statins depends on multiple clinical considerations including the totalcholesterol levels , LDL levels, HDL levels, history of previous myocardial infarction and other riskfactors for coronary artery disease, particularly diabetes. Statins have been shown to have a favorableeffect on the arteries irrespective of the degree of cholesterol lowering achieved. This effect is believedto be through an anti-inflammatory action resulting in stabilization of atherosclerotic plaque. Because ofthis, some studies have suggested that intensive, immediate statin therapy may be initiated for patientswho are hospitalized with coronary artery disease.

    Bile acid resins. Because the liver takes cholesterol out of the blood to make bile, bile acid resinsprevent the recycling of bile acids in the intestine. As a result, the liver is forced to remove morecholesterol from the blood in order to manufacture more bile. Bile acid resins are usually taken inpowder form or in a chewable bar. Many patients, however, have gastrointestinal discomfort with these

    drugs. Bile acid resins are also known to bind to other substances, such as fat-soluble vitamins, theheart drug digoxin and the anticoagulant warfarin. It is not recommended that patients take these drugsat the same time they are taking bile acid resins.

    Nicotinic acid (niacin), a form of vitamin B3. In large doses, nicotinic acid is very effective in loweringtriglyceride levels and raising levels of HDL (good) cholesterol. Nicotinic acid can also lower levels ofLDL (bad) cholesterol, but not as effectively as other cholesterol reducers. When taking niacin, patientsare advised to slowly build up to the high doses needed to treat high cholesterol. Taking too much niacincan lead to intense side effects that include flushing, palpitations, nausea and, in extreme cases, livertoxicity (especially when taken in rapid-release form). Even with proper build-up, as many as 50percent of patients find the side effects of this medication too difficult to tolerate. Nicotinic acid isavailable over the counter, but physicians prefer to prescribe it in time-released pills. Because of thepotentially intense side effects, patients should never begin taking niacin without the supervision of aphysician. Additionally, many of the "no flush" niacin dietary supplements sold over the counter do not

    affect blood lipid levels.

    Fibrates (or fibric acid derivatives). Fibric acid reduces the production of triglycerides and increases therate at which existing triglycerides are removed from the bloodstream. Fibrates can significantly lowertriglyceride levels and modestly increase HDL (good) cholesterol levels in most patients, but they areless effective at reducing LDL (bad) cholesterol levels. They are most commonly used in patients whohave elevated triglyceride levels, usually in conjunction with low HDLs (many diabetics have this type oflipid profile). Simultaneous use of fibrates and statins should be carefully monitored.

    Ezetimibe. Ezetimibe is a newer class of cholesterol drug that blocks cholesterol absorption in the smallintestine. It has been shown to reduce LDL cholesterol levels, although not as much as statins.Ezetimibe has been marketed alone and combined with statin drugs. The drug class was approved bythe U.S. Food and Drug Administration in 2004, but a clinical study released in 2008 indicated thatezetimibe alone or in combination provided no benefits that could not be achieved with a statin drug.

    One specific measure in the study (the thickness of plaques in carotid arteries) did not improve at alland, in some cases, appeared worsened by the drug.

    Potential side effects of cholesterol drugsThere are a number of side effects that could occur as a result of taking cholesterol reducers, but fortunately, sideeffect frequency is low. Muscle aches can occur with statin use and must be immediately reported to a physician.Certain cholesterol-lowering medications can also produce abnormalliver function in approximately 2 percentof the population, which can be diagnosed by periodic liver enzyme testing. In rare cases, this may lead to liverfailure. Patients with moderate or severe liver disease should not take statins. For the most part, abnormal liverfunction is reversible when the statin is discontinued.

    A rare, but potentially fatal side effect of some cholesterol-reducing drugs (statins and certain fibrates) isrhabdomyolysis, a severe muscle reaction in which muscle cells break down, releasing their contents into thebloodstream. Physicians can monitor patients for this complication by checking muscle enzyme levels (e.g.,

    creatine phosphokinase [CPK]) in the blood. It most often affects the muscles in the back or lower calves. Somepatients report no symptoms and in rare cases rhabdomyolysis can lead to kidney or other organ failure and

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    death. Patients should report any of the following symptoms of rhabdomyolysis to their physicians immediately:

    Muscle cramps, pain, swelling, weakness, stiffness and/or tenderness

    Fever

    Dark urine

    Nausea and/or vomiting

    Malaise (a general feeling of illness or discomfort)

    Risk of this severe complication appears to be higher in elderly patients, those taking high doses of statin andthose taking statins in conjunction with a fibrate (e.g., fenofibrate, gemfibrozil). In 2001, one type of statin, calledcerivastatin (brand name Baycol) was voluntarily withdrawn from the market by its manufacturer due to reportsthat fatal cases of rhabdomyolysis had been significantly more common with cerivastatin than with otherapproved statin drugs.

    Statins carry a very low risk of side effects to the nervous system, including tingling, numbness and burning pain.These manifestations are known as peripheralneuropathy.

    Patients on any cholesterol-lowering drugs should also notify their physician if they experience any side effectssuch as the following:

    Allergic reaction (new onset of wheezing, respiratory congestion, itching or skin rashes) Abdominal pain

    Headache

    Constipation

    Heartburn

    Dizziness or lightheadedness

    Flushing of the face or neck

    Bloating

    Blurred vision

    Drowsiness, weakness or fatigue

    Nausea or vomiting

    Hair loss

    Decreased sexual interest or ability

    Some cholesterol reducers can cause liver inflammation, which tends to resolve on its own after patients stoptaking the medication. To monitor this and other complications, patients will undergo regularblood tests andliver function tests.

    Women taking cholesterol-reducing drugs should inform their physicians at once if they are or plan to becomepregnant. Although it has been found that statins do not have a negative effect on female reproductive hormonelevels, cholesterol is an important contributor to the development of the fetus. In addition, some cholesterolreducers are excreted in breastmilk. Nursing mothers, therefore, should consult with their physician before takingor discontinuing these drugs. Patients should not abruptly stop taking their medications without first consultingtheir physicians. It is also important that patients notify all physicians (including dentists) that they are takingstatins before undergoing any surgical procedure. And all patients taking statins should inform their physicianimmediately of any side effects or concerns.

    Most patients on medication to treat high cholesterol (hypercholesterolemia) will be taking it for the rest of theirlives, provided no serious side effects occur. Patients should remember that medications may control highcholesterol, but they do not cure it. Even if all their symptoms are relieved, patients should continue to take theirmedication exactly as directed, eat a heart-healthy diet that is low in saturated fats and keep all scheduled follow-up appointments with their physician. Numerous studies have shown the dangers associated withnoncompliance, or people not taking their cholesterol-lowering medications exactly as prescribed. Even if themedications do not appear to make you "feel better," there is a significantly higherrisk of heart attack amongpeople who simply stop taking their medications.

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