The Five Faces of Statins

There is no doubt that the pharmaceutical industry would far prefer statin drugs to have but one face - reduction of cardiovascular risk. However, that was never the case and as long as these drugs are designed to attack the mevalonate pathway, never will be.

THE FIRST FACE (Cholesterol Reduction)
Though designed for reduction of cholesterol biosynthesis, a task they accomplish with great proficiency. Recent findings suggest that this face of statin drug effect is increasingly irrelevant to cardiovascular disease risk reduction.

Atherosclerosis, the underlying cause of heart attacks and strokes, is believed to be the result of inflammatory factors that may be associated with deficiencies of vitamin B6, 12 and Folic acid allowing abnormally high levels of homocysteine, the major player in atherosclerotic change, with coagulation defects, platelet factors and selected anti-oxidant deficiencies responsible for most of the rest and cholesterol no longer deserving even a place in the lineup.

THE SECOND FACE (Inhibition of NF-kB)
So now we know the second face of statin drugs, the effective face, the face that no doubt has prevented many cases of heart attacks and strokes.

No one seriously argues the positive effects of this happy face but it is anti-inflammatory, not cholesterol lowering. It is a face only recently recognized as the results of long-term studies have been analyzed. Whether your cholesterol goes up, down or sideways, statin drugs work by a means independently of cholesterol. This factor is nuclear factor-kappa B, a transcriptase common to our entire immuno-defense system.

The entire pharmaceutical industry has been shocked by this revelation but quick to acknowledge and adapt to the change for now statins are being promoted for organ transplant recipients and as adjunctive therapy in the treatment of auto-immune diseases. Why? Because they work! These results are sobering, indeed, for statin drugs can work in this capacity only at the risk of causing mischief elsewhere.

THE THIRD FACE ( Consequences of Immune System Effect )
So a third face of statin drugs has been added to its profile - the face concerned about that same nuclear factor- kappa B and its effect on the remainder of our immune system? What about cancer and infectious disease?

We have had 3.5 billion years to work out our defense systems against widely diverse challenges and NF-kB is key to all of them. Whether by being the recipient of a donor kidney or under attack by bacteria or viruses, or having a mutation induced by radiation in our environment, our immune system has evolved a defensive strategy in which suppression of inflammation, triggered by nuclear factor kappa B, plays a vital role. The ability of statin drugs to suppress this nuclear factor kappa B response is to open a veritable Pandora's Box of unpredictable consequences.

THE FOURTH FACE (Ubiquinone Deficiency)
Ubiquinone deficiency is the fourth face of Statins and the one responsible for the most severe side effects.
Statin drugs, while curtailing cholesterol, must inevitably inhibit the production of other vital intermediary products that originate further down the metabolic pathway beyond the statin blockade. The pharmaceutical industry has long been attempting to develop a means by which interference with cholesterol production might be achieved beyond the point where these vital intermediary products originate but up to now have failed. The inevitability of significant, serious and even lethal side effects has been knowingly accepted. Ubiquinone levels plummet when statins are initiated.

Such side effects as congestive heart failure and chronic fatigue reflects ubiquinone's important role in energy production. Hepatitis, myopathy, rhabdomyolysis and peripheral neuropathy reflect ubiquinone's role in cell wall integrity and stability. Ubiquinone's role in the prevention of somatic mitochondrial mutations also is of critical importance; Suffice it to say that it is, by itself, a vast area of concern.

THE FIFTH FACE (Dolichols)
The fifth face of statin drug effect has to do with dolichol availability. Like the ubiquinones, this class of compounds is collaterally damaged with statin drug use. Dolichols are involved in an intricate process of cellular activity involving message transport. Proteins manufactured there in response to DNA directives are packaged into transport vesicles that are shuttled across the cytoplasm to their various destinations.

Without dolichols there would be intracellular chaos as various proteins could not be directed to their proper target and would, in effect, be dead-lettered. The post office analogy, though childishly simple, comes very close to describing dolichol's function as it is understood today.

Since the discovery in 1975 of internally produced opiates, popularly described as Beta endorphins and finally labeled as neuropeptides, legions of scientists have explored the nature and role of these ubiquitous substances. Neuropeptides are biochemicals that regulate almost all life processes on a cellular level, thereby linking all body systems.

Although produced primarily in the brain, every cell in the body produces and exchanges neuropeptides, Called messenger molecules, they send chemical messages in the form of linked peptides from the brain to receptor sites on cell membranes throughout the body. Every thought, sensation and emotion we have ever felt has been dependent upon the makeup of these peptide linkages and they do not simply convey - these peptide clusters are the thought, sensation or emotion in a process we are only just beginning to understand.

It is strongly suspected that disruption of this system by statins is behind the reports of depression, hostility, aggressiveness, accident and addiction proneness and the many suicides soon after statin drugs are started.

Returning to the first face of statin, the cholesterol reduction face, it was only in 2003 that Pfrieger made his extraordinary breakthrough that defined for the entire world just how important cholesterol is to brain function. He found that cholesterol was the evasive substance for which his team had been searching for years, that synaptogenic substance responsible for the formation and function of our trillions of synapses as they service the neurons of our brains. He found that the glial cells of the brain provide for this cholesterol manufacture and of course are just as effectively inhibited by Statins and abruptly, only in 2003, there was finally an explanation for the bizarre cognitive side effects being reported.

Now there is a mechanism for the amnesia, confusion, disorientation, forgetfulness and aggravation of pre-existing senility. The findings of Muldoon claim that one can document cognitive deterioration in 100% of statin users with the right type of testing.

How strange it is that a class of drugs developed solely for the purpose of interfering with the biosynthesis of cholesterol has now been shown to reduce cardiovascular risk by an anti-inflammatory role completely unrelated to cholesterol manipulation.

We now have a nation of patients and doctors convinced that cholesterol is public health enemy number one for none of this recent truth has yet significantly penetrated the hallowed halls of health care delivery.
We have a pharmaceutical industry still committed to pushing the charade of cholesterol etiology. Imagine the billions of profit dollars resulting to them from perpetuating the myth of cholesterol and now when confronted by the reality of inflammation deftly turn their sights towards organ transplant and auto-immune disease.

Of the 2503 patients tested with Lipitor, seven experienced transient global amnesia attacks and four others experienced other forms of severe memory disturbances for 11/2503 or five cases of severe cognitive loss to result from every 1000 patients that took the drug, to come yet, not one word of warning of this was ever transmitted to the physicians who soon would be dispensing the drug.

Duane Graveline MD MPH
Former USAF Flight Surgeon
Former NASA Astronaut
Retired Family Doctor

Books From Amazon

The Dark Side of Statins
The Statin Damage Crisis
Cholesterol is Not the Culprit
Statin Drugs Side Effects
Lipitor, Thief of Memory

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