WARNING! Read These Before Taking Cholesterol Drugs

Statins and Your Cholesterol

Statins are the most popular drugs used to lower blood cholesterol levels. They are still commonly prescribed for people with hypercholesterolemia even though the first statin drugs were released over 20 years ago.

The sales of statin drugs are quite huge. Lipitor, the most popular statin drug, earned Pfizer over $12 billion in 2008 and has been determined to be the best-selling drug in history. Since the release of Lipitor (atorvastatin), newer generations of statins have been introduced as well as combinations with other cholesterol-lowering agents.

As cholesterol-lowering agents, statins inhibit the liver enzyme known as HMG-CoA reductase.

This enzyme is involved in the early stages of the mevalonate pathway. This is the synthetic pathway used for synthesizing cholesterol in the liver.

Statins are effective cholesterol-lowering drugs. They are especially effective for lowering LDL (low-density lipoprotein or “bad”) cholesterol levels. However, they are not as effective for reducing triglyceride levels or raising HDL (high-density lipoprotein or “good”) cholesterol as supplements such as niacin (vitamin B3).

Although they are commonly prescribed, statins are also controversial drugs with serious adverse effects and questionable benefits for reducing the risks of cardiovascular diseases.

An Overview of the Statin Controversy

An increasing number of scientists and doctors believe that statin drugs are overused. Although a number of large studies and reviews indicated that statins provided clear benefits, recent discoveries have revealed the shortcoming and biases of those trials.

For example, the JUPITER (Justification for the Use of Statins in Primary Prevention: An Intervention Trial Evaluating Rosuvastatin) trial is currently considered flawed.

This trial was done to investigate the benefits of rosuvastatin for reducing the risk of heart attacks and strokes in people with normal cholesterol levels. The researchers of the JUPITER trial concluded that statin drugs may prevent cardiovascular death in people other than those with high cholesterol levels.

This conclusion was used as a justification to expand the potential market of statin drugs.

After the JUPITER trial, doctors confidently prescribed statins not only for those with high blood cholesterol but also for those with normal blood cholesterol deemed to be at high risks of hypercholesterolemia.

However, reviewers now claim that this 2008 study is flawed and that the data gathered did not support the conclusions. Furthermore, the results of the JUPITER trial have been questioned because of the close involvement of the statin drug manufacturers.

The influence of statin manufacturers extends beyond the JUPITER trial. Evidence has also surfaced associating 8 out of the 9 doctors making up a National Cholesterol Education Program committee with drug companies. This committee recommended statins as the primary intervention and preventative measures for lowering blood cholesterol and reducing the risk of heart disease.

Since this recommendation, the market for statin drugs has tripled. Yet a review published in the journal, Lancet, pointed out that none of the studies examined by this committee supported its recommendation.

Adverse Effects of Statins

Quite a lot of studies have identified the various side effects of statin drugs and their severity. The most common adverse effect of this class of drugs is rhabdomyolysis and other forms of muscle and tissue degeneration.

Other side effects of statins include acidosis, anemia, nerve damage, cataracts, sexual dysfunction, memory loss as well as liver and pancreas dysfunction.

In addition, statins have been associated with increased risks of diabetes, cancer and Lou Gehrig’s disease.

Statins, CoQ10 and Muscle Weakness

The negative effects of statins on muscles are linked to a coenzyme known as CoQ10. This coenzyme is a cofactor for different enzymes and it is essential for the production of ATP (adenosine triphosphate), the chief energy molecule of cells.

Statins deplete the levels of coenzyme Q10 inside cells. This leads to reduced production of ATP and, therefore, impaired cellular metabolism.

The depletion of CoQ10 means that muscles with high energy requirements get weaker as ATP production drops.

While this fall in energy production causes muscle fatigue and weakness, it may also cause cardiovascular problems when the muscles of the heart are affected.

Coenzyme Q10 is also a natural antioxidant that helps mop up free radicals in the body. When statins deplete the body’s store of this coenzyme, harmful free radicals may accumulate and damage cells and DNA.

Of the statins, cerivastatin depletes coenzyme Q10 the fastest and, therefore, carries the highest risk of rhabdomyolysis. This is why it was withdrawn in 2001.

Although the risk of muscle damage is lower for other statins, it becomes significant at high doses and when they are combined with other cholesterol-lowering agents.

Because statins lower the levels of coenzyme Q10, experts advise that CoQ10 supplements should be taken along with statins.

Ubiquinol is the most effective form of coenzyme Q10. Doses lower than 200 mg are recommended to prevent muscle damage. However, to relieve statin-induced muscle weakness, 200 – 500 mg of the supplement is recommended.

Statins and Diabetes

Studies have shown that statins can increase the risk of diabetes. Although the FDA (Food and Drug Administration) believed that this risk is small and outweighed by the benefits of statins, it recently mandated that statins must carry black label warnings about their effects on blood sugar levels.

The FDA also acknowledged that statins can cause reversible memory loss and mental confusion although it no longer recommends regular liver function tests for statin users.

Past studies identified that statin can affect blood sugar control. These cholesterol-lowering drugs have been linked with type 2 diabetes especially when taken in high doses and when taken by those with elevated blood sugar levels.

Statins increase the risk of type 2 diabetes by 2 major mechanisms. First, they cause insulin resistance. Secondly, they raise blood sugar levels directly.

By promoting insulin resistance, statin drugs reduce the sensitivity of cells to blood sugar. Therefore, the amount of sugar in the blood rises while cells are starved of a major energy source.

The body removes excess sugar from the blood and stores it in the liver. The liver then converts the excess sugar into cholesterol and triglycerides. Because statins interfere with the synthesis of cholesterol in the liver, the excess sugar is returned back to the blood when it is not converted to cholesterol.

Statin-induced diabetes is actually different from type 2 diabetes because it is really a state of hyperglycemia.

For most people, blood sugar levels will revert back to normal when statin use is discontinued.

Experts believe that the rising incidence of diabetes in the population may be partly explained by the indiscriminate prescription of statin drugs.

In some cases, doctors prescribe statins to diabetes patients because they believe the benefits outweigh the risks.

However, studies demonstrate that the effects of statins on blood sugar control are worse in diagnosed diabetics. Therefore, another cholesterol-lowering drug besides statins may represent a better treatment choice for diabetics with heart problems.

More Than Cholesterol

As HMG-CoA reductase inhibitors, statin drugs act very early in the synthesis of cholesterol. More specifically, they inhibit the conversion of HMG-CoA (3-hydroxy-3-methylglutaryl-CoA) to mevalonic acid.

There are quite a number of metabolic steps between this reaction and the eventual production of cholesterol from lanosterol. Therefore, in order to inhibit cholesterol synthesis, statins block the production of a number of intermediates used to synthesize other important natural compounds in the body.

Some of the natural compounds affected by the statin blockade of cholesterol synthesis include all sterols, sex hormones, dolichols, and cortisone.

Dolichols are needed to maintain the integrity of cell membranes. Sterols are used in multiple physiological processes and serve as precursors for other important compounds. For example, one of the sterols blocked by statin drugs is a cholesterol metabolite needed in the synthesis of vitamin D in the skin.

Therefore, statin drugs impair the body’s ability to produce vitamin D. Since studies have shown that vitamin D can help improve insulin resistance, this impairment of vitamin D resistance may be one of the mechanisms by which statins induce diabetes.

The broad range of statins’ adverse effects is understandable given the number of precursors blocked by the inhibition of HMG-CoA reductase by these drugs.

It is difficult to completely document the extent of the damage caused by this enzymatic inhibition since biochemical reactions are closely linked together. But it is safe to assume that this inhibition will cause wide-ranging negative effects in different organs and systems of the body.

With the knowledge that statins are dangerous drugs with far-reaching consequences, it is only right to wonder what benefits they provide and who exactly benefits from statins given its steep risk-reward ratio.

Statins and the Truth About Cholesterol

Doctors are quick to recommend statins for lowering blood cholesterol and statin manufacturers aggressively market those drugs. This combination has resulted in the overuse of statin drugs even though experts agree the most users do not need statins.

The truth is that there are natural and effective means of improving the blood lipid profiles.

Statins are only really needed for cases resistant to natural remedies such as the ones caused by the genetic defect known as familial hypercholesterolemia.

However, statin manufacturers have greatly benefited from the victimization of cholesterol in public health. Contrary to popular belief, total blood cholesterol is not the root cause of heart disease.

Cholesterol is not bad for health. In fact, there are people with high blood cholesterol (over 250) who have low risks of heart disease. There are also people with low blood cholesterol (under 200) with a high risk of heart disease due to their low HDL cholesterol level.

The truth is that cholesterol is essential for a number of biological processes including the production of sex hormones, bile acids, cell membranes, and vitamin D.

What happens to the cholesterol in the blood determines its fate and its effects on cardiovascular health.

Therefore, total blood cholesterol is not a true indicator of the risks of atherosclerosis and heart failure. There are better predictors of these risks. They include the ratio of HDL cholesterol to total cholesterol and the ratio of triglyceride to HDL cholesterol.

Creating New Markets for Statin Drugs

Even though clinical data show that 1 in 4 adults over the age of 45 are already taking a statin to lower blood cholesterol levels and reduce the risk of heart disease, very few are aware of most of the serious adverse effects of this class of drugs.

For example, one of the little-known side effects of statins is their teratogenic effects. Statin use can cause fetal malformations when taken by pregnant women.

Unfortunately, not all doctors recognize this risk. This has led to the increased prescription of statins for pregnant patients.

Although statins are classified under Category X medications, the marketing power of Big Pharma has overshadowed the dangers of these drugs so much that doctors are unknowingly increasing the risks of birth defects by prescribing more statins.

Much as giving statins to pregnant women looks bad, the new move by Big Pharma to encourage doctors to prescribe statins for children is even worse.

Even as the patent for Lipitor expired in late 2011, Pfizer was introducing a new demographics to its best-selling drugs. The release of a chewable formulation of Lipitor is lined up to fulfill the anticipated demand generated by certain health experts calling for cholesterol screening in schools in a half-hearted bid to combat childhood obesity.

Prescribing statins for children may turn out to be one of the worst failures in public health.

With known adverse effects ranging from muscle wasting and organ failure to cognitive decline and diabetes, it is difficult to justify giving statins very early in life. Exposing the body to statins very early will definitely increase the incidence of chronic diseases later in life.

How to Naturally Improve Your Cholesterol Profile

Drugs such as statins are not the only effective way to lower your “bad” cholesterol and raise your “good” cholesterol.  Some of the effective natural supplements that can help improve your lipid profile are listed in the table below.

In addition, you should adopt lifestyle changes including eating more heart-healthy foods low in fats and cholesterol. Regular exercise is also highly recommended for improving your cholesterol profile.

Make sure to avoid refined foods especially simple sugars. Avoid excessive consumption of alcohol and stop smoking.