Statins: Cholesterol Medication

Statins also known as cholesterol medication are a class of pharmaceutical drug that inhibit the production of an enzyme called HMG-CoA reductase. This mechanism of action also makes Statins hypolipidemic or blood fat reducing. The primary use of these drugs is for cholesterol management.

Inhibition of the HMG-CoA reductase enzyme in the liver stimulates LDL cholesterol receptors. This increases elimination of low-density lipoprotein - LDL from the bloodstream followed by an overall decrease in blood cholesterol levels.

HMG-CoA reductase is a key enzyme in the cholesterol synthesis pathway.

Cholesterol Synthesis Pathway

The onset of the drug's effect is quite rapid...initial results can be documented in blood tests in a week or so...the full effect can be seen by six weeks.

Statins are particularly effective at lowering LDL cholesterol levels...typically anywhere between 20% - 50%. LDL has become well known as 'bad cholesterol' although it is a very necessary component of your blood chemistry. The problem with LDL cholesterol is that it can cause inflammation in the arterial wall if it becomes oxidised.

These drugs can also reduce elevated triglyceride levels and produce a modest increase in HDL-cholesterol.


Over 100 years ago a German pathologist discovered that cholesterol was to be found in the artery walls of people that died from myocardial infarction. It was thought that the presence of the cholesterol was instrumental in the thickening process of the inside of the wall of the artery that lead to it narrowing or blocking.

In the 1950's the famous Framingham heart study found a statistical relationship between elevated cholesterol levels and Coronary Heart Disease.

As a result of the Framingham findings researchers began to investigate possible ways to interfere with the body's own cholesterol production process.

In the 1970's A Japanese microbiologist - Akira Endo happened on an inhibitor of HMG-CoA reductase while researching antimicrobial agents. He found that a specific type of Penicillin exhibited this quality. Clinical trials though revealed higher than expected toxicity levels.

In the late 1970's pharmaceutical company researchers found that a particular species of fungus successfully interfered with the cholesterol synthesis pathway. A product mevinolin was born which became known as lovastatin.

Some common examples of Statins are...

  • Lovastatin - Mevacor
  • Atorvastatin - Lipitor
  • Fluvastatin - Lescol
  • Rosuvastatin - Crestor
  • Simvastatin - Zocor
  • Pravastatin - Pravachol

Possible side effects may include...

  • headache
  • constipation
  • diarrhea
  • nausea
  • vomiting
  • muscle pain
  • weakness
  • rash

A very serious side effect of statins can be the onset of a condition called Rhabdomyolysis.

Rhabdomyolysis occurs with the breakdown of muscle fibers which results in the release of myoglobin - a muscle protein into the bloodstream. This is toxic to the kidneys and can result in kidney damage.

Symptoms of Rhabdomyolysis may include...

  • Abnormal urine color
  • Muscle stiffness or aching - Myalgia
  • Muscle tenderness
  • Weakness of the affected muscles
  • Fatigue
  • Joint pain

Cholesterol medications can interact with some other Pharmaceutical drugs that you may have been please make sure that you fully inform your health care professional.

Grapefruit and Statins:

A potential interaction that may surprise you is that of grapefruit and statins. Some compounds in grapefruit juice can interfere with the enzymatic breakdown of the statin drug. This can lead to an accumulation of drug in your body with all the risks and side effects that are associated with that.

To avoid this potential hazard, don't consume grapefruit juice at the same time as you take your medication.

Concerns with the widspread use of Statins:

In my opinion , the widspread use of statins in healthy individuals may be unwise. Statins inhibit synthesis in the liver of other important chemicals besides the desired target of cholesterol reduction.

Ubiquinone or CoEnzyme Q10 is one of three important end points in the chemical synthesis chain that also produces cholesterol and the use of these drugs will inhibit its production

Coenzyme Q10 is involved in the process of cellular energy production, acts as an antioxidant, supports healthy heart muscle function and may help protect LDL cholesterol from the oxidation process.

I don't know anyone taking statins that was advised to supplement with CoQ10...clearly if your body's ability to produce this important chemical is being depressed then supplementation is of prime importance.

What about drug trial data?

An analysis of the data generated by several major statin drug trials carried out before the year 2000 found that long-term use...and that's what we want to know...for primary prevention of heart disease - that is - people who have not yet been diagnosed with heart disease but are taking these drugs to reduce that risk, produced a 1 percent greater risk of death over a 10 year period compared to a placebo...interesting, not to mention surprising.

These findings were published in the British Journal of Clinical Pharmacology in 2001.

Pharmaceutical company funded study data can be interpreted creatively in order to maximize the sale of a product. I advise that you do your research here before blindly accepting advice to take a pharmaceutical drug that you may not need and which could harm your health in the long term.

What about Statins and Familial Hypercholesterolemia?

If lab tests have confirmed that you have familial hypercholesterolemia - an inherited condition that causes very high blood cholesterol levels, there may be no other viable alternative in the short term but to try statin drugs for a period...(although you will no doubt be told you have to stay on them indefinitely). While you do this, work towards some radical lifestyle changes that must include...

  • serious diet modification - including the adoption of low glyceamic eating and drinking
  • daily physical activity and relaxation
  • address and modify all your other Coronary Disease risk factors
  • stress reduction and...
  • quality real food dietary supplementation

Blood sugar and HMG-CoA reductase activity:

HMG-CoA reductase is active when blood glucose is high. Controlling blood sugar levels can indirectly affect the activity of HMG-CoA reductase.

Insulin - the hormone that the body produces in response to high blood levels of glucose encourages the production of cholesterol because it has a stimulating effect on HMG-CoA reductase.

Maintaining healthy blood sugar levels by eating and drinking food items that are low glyceamic can help to control the amount of cholesterol your liver synthesizes.

A low glycaemic food is typically one that has a high fiber content thereby allowing a more progressive break down of the food in your digestive system...releasing any sugars at a slower rate thus helping to avoid the spiking of insulin levels.

Find a health care professional that will work with you to reduce your cholesterol medication dose over time...see how far you can lower your cholesterol level by increasingly relying on lifestyle modifications to assist you.

If you do not have familial hypercholesterolemia then after discovering that your cholesterol level is elevated, proceed straight to lifestyle modifications. A cholesterol drug or statin should be last on your list...unless you're happy to accept the risks of course.

Click here to go from Statins to Heart Drugs

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