Cholesterol Reduction :: A Doctor's Guide
Cholesterol Reduction

Medication to Lower Cholesterol

Lowering the levels of fats (lipids) in the blood, including cholesterol and triglycerides is the basic function of the cholesterol reducing drugs. High levels of these fats in the bloodstream increase the risk of hardening of the arteries (atherosclerosis), heart attack, stroke and other heart-related conditions. Therefore, cholesterol reducers and other antilipemic medications are often prescribed for people with high cholesterol levels (hypercholestolemia) or other elevated lipid levels (e.g., high triglycerides).

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

Researchers have also identified new forms of cholesterol, called non-HDL cholesterol. This group includes VLDLs (very low-density lipoproteins) and intermediate-density lipoproteins (IDLs). Both categories have been linked to increased risk of non-fatal heart attack and angina among individuals who already have heart disease and may be treated with cholesterol lowering drugs.

It has also been suggested that cholesterol-reducing drugs can benefit patients with coronary artery disease who have an implantable cardioverter defibrillator (ICD). Studies suggest that cholesterol-lowering therapy may have an anti-arrhythmic effect, resulting in fewer recurring episodes of ventricular tachycardia and ventricular fibrillation and a decreased need for automatic firing of the ICD.

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

Different opinions regarding the conditions and the way the drugs work on the human body vary. Some are optimistic, some are pessimistic and some outright cynical. But it is for you to make a wise decision in consultation with your doctor whether he is biased towards a particular treatment. Studies show that different types of cholesterol reducers affect levels of fats (lipids) in different ways and generally fall into the following categories:

Statins: Considered as the first line of treatment for most patients with high cholesterol (hypercholesterolemia), statins block the production of specific enzymes used by the body to make cholesterol. Statins have been shown to reduce the risk of a first heart attack, as well as recurrent heart attacks in patients with known disease. They 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. Statins generally have limited side effects, although there are some reports of a rare muscle deterioration called rhabdomylosis. Some media reports have also linked statins to reduced memory function, but this appears 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 total cholesterol levels, LDL levels, HDL levels, history of previous myocardial infarction and other risk factors for coronary artery disease particularly diabetes. Statins have been shown to have a favorable effect on the arteries irrespective of the degree of cholesterol lowering achieved. This effect is believed to be through an anti-inflammatory action resulting in stabilization of atherosclerotic plaque.

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

Nicotinic Acid (Niacin) is a form of vitamin B3. In large doses, nicotinic acid is very effective in lowering triglyceride levels and raising levels of HDL ("good") cholesterol. Nicotinic acid can also lower levels of LDL ("bad") cholesterol, but not as effectively as other cholesterol reducers. When taking niacin, patients are advised to slowly build up to the high doses needed to treat high cholesterol. Taking too much niacin can lead to intense side effects that include flushing, palpitations, nausea and, in extreme cases, liver toxicity (especially when taken in "rapid-release" form). Even with proper build-up, as many as 50 percent of patients find the side effects of this medication too difficult to tolerate. Nicotinic acid is available over the counter, but physicians prefer to prescribe it in time-released pills. Because of the potentially intense side effects, patients should never begin taking niacin without the supervision of a physician.

Fibrates (Or Fibric Acid Derivatives): Fibric acid reduces the production of triglycerides and increases the rate at which existing triglycerides are removed from the bloodstream. Fibrates can significantly lower triglyceride levels and modestly increase HDL ("good") cholesterol levels in most patients, but they are less effective at reducing LDL ("bad") cholesterol levels. They are most commonly used in patients who have elevated triglyceride levels, usually in conjunction with low HDLs (many diabetics have this type of lipid profile). Simultaneous use of fibrates and statins should be carefully monitored.

Ezetimibe: Ezetimibe represents a new class of drug that directly blocks cholesterol absorption in the small intestine (in contrast to bile acid resins, which bind with bile acid in the intestine). Ezetimibe is most commonly used in addition to statins, whereby up to an additional 25 percent reduction in LDLs is achieved. It can also be used as a single agent. Side effects have shown to be similar to that of placebo, and there is minimal increase in liver enzymes when used with statins.

Examples of the above medications include the following:
  • Statins
    • Atorvastatin
    • Fluvastatin
    • Lovastatin
    • Pravastatin
    • Rosuvastatin
    • Simvastatin
  • Bile Acid Resins
    • Cholestyramine
    • Colestipol
    • Colesevelam
  • Nicotinic Acid
    • Niacin (Vitamin B3)
  • Fibrates
    • Clofibrate
    • Fenofibrate
    • Gemfibrozil

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