Statins – The Basics
Statins – The Basics
The statins (or HMG-CoA reductase inhibitors) are a class of drugs that lower cholesterol levels. The first results can be seen after one week of use and the effect is maximal after four to six weeks.
- Simvastatin – Zocor – available over the counter in the UK
- Cerivastatin – withdrawn after killing too many people/muscle disintegration
- Atorvastatin – Lipitor – highest sales
- Rosuvastatin – Crestor
How statins lower cholesterol levels:
- Lower cholesterol synthesis in the liver
- The liver starts to run out of cholesterol to make VLDLs
- The liver increases the number of LDL receptors to pull cholesterol back to make more VLDLs
- LDL is dragged back to the liver, hence
- LDL levels in the blood fall
The blood-brain barrier (BBB)
- is a metabolic or cellular structure in the central nervous system (CNS) that restricts the passage of various chemical substances and microscopic objects (e.g. bacteria) between the bloodstream and the neural tissue itself, while still allowing the passage of substances essential to metabolic function (e.g. oxygen).
- it also stops cholesterol from entering the brain in the blood, hence the brain produces its own cholesterol for proper brain functioning.
- But it does let statins through which inhibit cholesterol production in the brain.
Coronary Heart Disease (CHD) – not caused by cholesterol levels but inflammation of the artery walls, which may be caused by (but not known);
Cholesterol levels are an indicator of risk of CHD in middle aged men, but not the cause of CHD.
Statins – they seem to work to reduce CHD but not due to lowering cholesterol – probably work by reducing inflammation of the artery
- Cause muscle pains and muscle weakness in up to 20% of people who take them
- Cause memory loss, depression, confusion, irritability and dizziness
- Cause rhabdomyolysis (breakdown of muscle) which can be fatal
- Cause polyneuropathy (a neurological disorder that occurs when many peripheral nerves throughout the body malfunction simultaneously)
St Thomas Hospital London – 36% of patients on 80mg Lipitor noted side effects.
Lipitor‘s TNT trial implodes: 5000 heart patients for 5 years on 80 mg top-dose suffer 2 more deaths than patients on only 10 mg.
Reduce inflammation of the artery linings naturally by:
- Avoid trans-fats (made by heating all vegetable oils)
- Avoid Refined sugars & refined fructose
- Avoid reduced fat milk – contains oxidised cholesterol which irritates the artery wall.
- Take Cod liver oil (vitamin A, D and EPA)
- Eat saturated fat
- Take evening primrose oil – sources of GLA
- Eat liver – high in copper
- Eat coconut oil – protect against bacteria & viruses
Cause of Statin Side Effects:
The reasons for statin drug side effects are better appreciated by using this figure of the Mevalonate Pathway ( also known as the HMG-CoA reductase pathway ) adapted from any medical school biochemistry book.
All statins are reductase inhibitors and therefore exert their effect at the very beginning of the mevalonate pathway, the location of this key reductase step. When statin drug manufacturers make the claim of reduction of cholesterol synthesis, it is based upon inhibition of the mevalonate pathway, shared by the other major elements such as CoQ10 and dolichols.
Statins act by inhibiting HMG-CoA reductase as indicated in this figure. All metabolic functions further down the pathway are consequently affected.
1) Cholesterol Inhibition
Not only is glial cell cholesterol synthesis in our brains vital for memory function and cognition, cholesterol also is the substrate for our most important homones: aldosterone, cortisone, estrogen, progesterone and testosterone as well as the quasi-hormone, vitamin D (calcitrol). Cholesterol’s vital role in membrane structure and function and lipid raft formation, makes it of critical importance in cell identification, cell communication and immunodefense.
Glial Cell Inhibition Potential Side Effects:
Confusion Disorientation Increased Senility
Hormone Lack Potential Side Effects:
Loss of Libido ( sexual desire )
Erectile Dysfunction ( ED)
2) CoQ10 ( Ubiquinone ) Inhibition
Coenzyme Q10 (CoQ10) is important for structural integrity of cells, anti-oxidation and, as part of the mitochondria, the production of Adenosine Triphosphate ( ATP ) energy. Part of its extreme importance in anti-oxidation is because of its location within the mitochondria, protecting the delicate components of the mitochondria from excess oxidative change and mutation.
Lack of Energy Potential Side Effects:
Chronic Fatigue Syndrome
Congestive Heart Failure
Shortness of breath
Loss of Cell Wall Integrity Potential Side Effects:
Myopathy ( muscle pain and weakness, cramps )
Peripheral Neuropathy ( numbness, tingling or burning sensations particularly in hands and feet )
Rhabdomyolysis ( rapid breakdown of skeletal muscle tissue )
Excessive Oxidation Potential Side Effects:
3) Dolichol Inhibition
Dolichols are vital to the process of glycoprotein formation in the endoplasmic reticula of cells. In this capacity it is critical to the formation of the glycoproteins involved in neuropeptides, cell identification, cell messaging and immunodefense. Reduced bioavailability of dolichols can affect every cellular process in the body.
Neuropeptide Dysfunction Potential Side Effects:
Altered Glycoprotein Synthesis Potential Side Effects:
Impairment of DNA error correction
Dysfunction of almost any cellular process
Altered cell identification
Altered cell messaging
4) Tau Protein Synthesis
When normal phosphorylation is interfered with by mevalonate blockade, our cells increase the production of Tau protein. Tau is the protein substance of the neurofibrilatory tangles common to Alzheimers and other neurodegenerative diseases.
Neuro-Degenerative Diseases Include:
Amyotrophic Lateral Sclerosis ( ALS )
Primary Lateral Sclerosis ( PLS )
Multiple Sclerosis ( MS )
Multiple System Atrophy ( MSA )
Frontal Lobe Dementia
Only recently discovered were selenoproteins and the effect of statin blockade of the mevalonate pathway on their role in human physiology. Deficiency of selenoproteins has been proven to result in various types of myopathies formerly seen only in areas known to be deficient in this trace element. Additionally cognitive dysfunction is known to be associated with selenium lack.
6) Nuclear Factor – kappa B (NF-kB)
The benefit of statin drugs in cardiovascular disease control is in their ability to inhibit this vital transcriptase. The entire anti-inflammatory and immunomodulatory effect of statins is mediated by statin inhibition of nuclear factor-kappa B. Improvement in atherosclerosis results from the inhibition of the key inflammatory elements: smooth muscle migration. lymphocyte adhesion, macrophage attraction and platelet activation associated with inhibition of NF-kB. The immunodefense system is also keyed to NF-kB, explaining the changing patterns of certain infections and cancers. The rise in cancers of all kinds secondary to statin use is of major concern.
Duane Graveline MD MPH
Former USAF Flight Surgeon
Former NASA Astronaut
Retired Family Doctor