• How To Stay Out Of Trouble When Taking Dietary Supplements

    Posted March 28, 2013: by Bill Sardi

    In this modern era when the usage of dietary supplements is popular and growing (U.S. supplement sales rose 7 percent to $11.5 billion in 2012, and are forecasted to reach $15.5 billion by 2017), and there is a strong upsurge in the use of vitamin D (up from $40 million in 2001 to $425 million in 2009), calcium ($177 million sales in 2012) and polyphenols (green tea catechins, grape seed proanthycyanidins, red wine resveratrol, curcumin from turmeric spice, silymarin from milk thistle, many others), unguided use is resulting in many avoidable side effects.  (Herbal supplement sales were $5.3 billion in 2011.)

    Don’t get me wrong.  Dietary supplements antagonists unwaveringly pitched against dietary supplements are sure to misquote what I am saying and launch their “I told you so” reports.

    Dietary supplements are safer than tap water, aspirin, vaccines and even table salt.  Poison control center data confirms dietary supplements are safe.

    The side effects I’m talking about usually cause supplement users to back away from their use.  But there are also some long-term threats posed by improper supplement use that are not so apparent in the short term and need to be addressed.

    The above-mentioned supplements, when used skillfully, are at the center of a self-help health revolution that surely will reduce mortality rates and hold promise to prolong the healthspan of many millions of Americans.  However, their improper use often emanates from over-enthusiast use and the mistaken notion that more is better.

    A key problem is that even supplement-savvy physicians are not well trained in the use of dietary supplements. Many supplement users don’t disclose what they are doing to their family physician for fear of being subjected to ridicule.  One survey revealed about a third of supplement users don’t inform their doctors of the dietary supplements they use, but the real figure is probably much higher.

    Unfortunately medical school usually leaves physicians with common biases against dietary supplements.  Some of these misconceptions are: vitamin A can be toxic to the liver — yes, but mostly among alcoholics and patients with pre-existing liver disease; vitamin C causes kidney stones – based on contrived science; vitamin D can induce hyper-calcification – yes, but at doses in excess of 1 million units in the animal lab; vitamin E can over-thin the blood – disproven by modern studies; magnesium induces diarrhea – yes but it is an effective laxative, and it induces loose stool, not expulsive diarrhea.

    When it comes to nutritional supplements, doctors can be generally categorized as dumbbells, (even though supplements have a high rate of use among health professionals) whose entire scope of nutritional expertise often doesn’t extend beyond the recommendation of an aspirin tablet, a Centrum multivitamin and a calcium pill.

    I may be a relentless advocate of dietary supplements, but they aren’t totally without side effect and safe at any dose.  It is unconscionable to think that the supplement industry is in some cases mistakenly circling its wagons to blindly defend dietary supplements largely because of the income stream they now generate.  Calcium supplements are the biggest example.

    Calcium pills:  yea or nay?

    My argument against supplemental calcium for post-menopausal women first appeals to common sense.

    I ask women who no longer have monthly cycles, as they began to approach menopause they developed a nutrient shortage of ________?  They usually answer “calcium.”

    I say no, let’s do this again.  As menopause sets in you develop a deficiency of  _______ ? They have no clue.  They look at me dumbfounded.

    So I answer it for them: “estrogen.”

    “Oh, ya, the ovaries stopped producing hormones,” they say.  Seems obvious, doesn’t it?

    And estrogen sends a signal to hold calcium in bone.  Lose that signal and it doesn’t matter how much calcium you pour into your body it will leach out and be deposited in your arteries, stiffening them like a statue.

    The more bone that is lost, the more that arteries are progressively diseased.  That is why a growing number of published studies now say supplemental calcium increases the risk for mortal heart attacks!  High dietary consumption of calcium (1400 mg) coupled with calcium supplements has been found to increase the risk for death from all causes by 257%.  Supplemental calcium below 500 mg didn’t pose a risk.

    Supplement industry in denial

    The supplement industry is in denial over this.  The Council For Responsible Nutrition, which represents supplement makers, refers to the Institute of Medicine recommendation for women over age 50 to consume 1200 mg of calcium.  But that number is the amount of calcium from the diet plus supplements.  The typical American diet provides 800-1200 mg of calcium.  So only small amounts of supplemental calcium are needed, if at all.  The problem is the inability to retain calcium in bone, not a lack of intake.

    Furthermore, since the loss of calcium from bone is not being addressed, this is why supplemental calcium is like pouring calcium into a barrel with a hole in its bottom.

    So what modern medicine has done since frightening women away from hormone replacement therapy is to increase the risk of hip fracture by 55%.

    What happened in the aftermath of advice to avoid hormone replacement therapy was that alternative therapies (bone hardening drugs) were recommended which pose some of the same health risks as estrogen.  Some investigators think modern medicine took one step forward and two steps back when it backed away from estrogen replacement.  Bottom line, estrogen replacement therapy is as safe as what has been recommended as an alternative.

    Health authorities now concede that restrictions on hormone replacement therapy are not supported by the original data used to make that recommendation.

    Estrogen replacement not only helps retain bone integrity but also inhibits deposition of calcium that stiffens arteries.

    In lieu of estrogen replacement, fearful women who don’t want hormone therapy, may opt for use of weak plant estrogens like resveratrol (rez-vair-ah-trol), known as a red wine molecule, that is 1/7000th the strength of natural estrogen but acts like estrogen to retain calcium in bone.

    Women can supplement their diet with all of the calcium, magnesium, vitamin D, strontium, and other bone enhancing nutrients they want, but unless the estrogen signal is replaced to hold calcium in bone, bones will continue to wither.

    Vitamin D and vitamin K are effective anti-calcifying agents that may be helpful, but they do not replace estrogen.

    Use of supplemental vitamin D and K help to reduce bone fracturesVitamin D in higher doses than have been recommended may be needed. Both vitamin D and K not only aid in retaining bone strength, but also help maintain elastic (un-calcified) arteries.

    Bottom line: Don’t fall for all the sales pitches to drink more calcium-rich milk or take calcium pills, even if given by your doctor.

    Another tip for women facing bone loss and accompanying loss of physical stature– without sleep, bone is lost.  Women with low estrogen levels report many sleepless nights.  This points to the importance of another hormone, melatonin.  When animals had their pineal glands removed, which secrete melatonin, their bones rapidly withered.  Sleep is of great importance for bone health.  Nighttime is when the bones repair and rebuild.  The ideal time to take bone supplements is at bedtime and a melatonin tablet may be a beneficial addition to your bone-building regimen.  Some bone-enhancing dietary supplements now provide low-dose calcium with vitamin D and melatonin with the recommendation they be taken at bedtime.

    Vitamin D: balance it with vitamins A and K and calcium/ magnesium

    Millions of Americans have begun to take vitamin D pills given an upsurge of published reports that low vitamin D levels are linked to a number of maladies.

    I was recently interviewed on a nationwide radio program and received many inquiries about leg spasms, toe curling and foot cramping.  I wondered what could be causing these muscle cramps.

    I can remember, as a teenager, returning from a day at the beach and experiencing the worst charley-horse cramps in my leg muscles.  A day in the bright sun had produced high vitamin D levels that increase the utilization of muscle-constricting and relaxing minerals such as calcium and magnesium.  An imbalance of these minerals can produce excruciating leg and foot cramps.

    Having adopted vitamin D3 pills into my daily supplement regimen I began to experience leg cramps and my toes began to tighten and curl in bed.   I found a low-dose calcium/magnesium supplement helped relieve this problem.  Maybe a reduction in the dose of supplemental vitamin D will also eradicate these muscle cramps.

    Another lesson I learned about vitamin D is that it is stored in the liver as a fat-soluble vitamin along with vitamin A and vitamin K.  Too much vitamin D can impair liver storage of vitamin A.  I don’t consume butter or other vitamin A-rich foods on a regular basis, mostly relying on my diet and supplements to provide vitamin A converted from beta carotene in carrots, squash, etc.

    As time passed I experienced two eye infections within a short period of time.  I had never had an eye infection in my lifetime.  My eyelids were also sticky when I awoke in the morning.  I gave this some thought and wondered if I was getting enough vitamin A to produce mucin that coats the surface of my eyes.  Mucin serves as a barrier against infection.

    So I laid my vitamin D pills aside and began to take cod liver oil as a natural source of vitamin A and my sticky eyelid problem disappeared and I have not had another eye infection.  I now supplement my diet with vitamin A-rich cod liver oil two days a week and vitamin D 5 days a week.

    By the way, cod liver oil provides such a miniscule amount of vitamin D that it cannot be relied upon as a source of this vitamin.

    It’s also important to know that all of the alleged side effects of high-dose vitamin D appear to emanate from a shortage of vitamin K.  So vitamin K2 supplements are suggested as a way to balance these fat-soluble nutrients.  Some vitamin D formulas now include vitamin K.

    Bottom line, balance out your vitamin D with vitamins A and K.

    Here come the polyphenols  (pall-ee-fee-nols)

    A class of molecules called polyphenols (also known as bioflavonoids), derived from citrus rind, berries, tea leaves, grapes, pomegranate, spices, coffee beans pose the greatest threat to modern pharmacology.  There is no biological challenge too great for them to conquer, ranging from cancer, brain disease, mood problems, infection, inflammation, heart disease and even obesity.

    Polyphenols activate a wide array of genes, more than man-made drugs, as they are small molecules that can get into the genetic machinery within cells.

    Polyphenols exert a broad range of biological effects as antioxidants, metal chelators, antidepressants (MAO inhibitors), anti-bacterial, anti-fungal, anti-viral agents, anti-inflammatory factors, etc.  In fact, they are many drugs in one.  They work synergistically when combined.

    As dietary supplements they are popularly consumed as curcumin from turmeric spice, quercetin from red apple peel, catechin from green tea, caffeic and chlorogenic acid from coffee beans, silymarin from milk thistle, and resveratrol from grapes and wine.

    These molecules from citrus, berries, herbs and spices work best in modest doses, as they are actually biological stressing agents.  As such, they are detected by the body as a biological threat and in response, activate internal antioxidant defenses.

    The dose is the poison

    This protective effect is only achieved when modest doses are consumed.  This phenomenon is known as hormesis.  It works by activation of a gene transcription factor called Nrf2 that increases the activity level of antioxidants produced internally in the body (glutathione, catalase, superoxide dismutase).  Pharmaceutical companies are now attempting to develop synthetic drugs that rely on a hormesis effect.

    However, as consumers learn about these promising polyphenolic medicines and incorporate them into their dietary supplement regimens, they aren’t hearing any precautions about dosage.  Excessive dose negates the proposed beneficial effects and may even worsen existing conditions.

    High herbal anxiety

    Investigator Ken Eagle notes that polyphenols in the diet and supplements inhibit an enzyme that keeps a lid on stress hormones released by the adrenal glands.  Sulfotransferase-1 is the enzyme that degrades adrenaline (aka epinephrine and norepinephrine).  Without this enzyme, stress hormones can run wild and induce headaches, insomnia, over-eating, elevate blood pressure, provoke heart palpitations, anxiety and even panic attacks.

    Polyphenols don’t cause stress hormones to be produced, but they may, if taken in large doses, inhibit the activity of a key enzyme that limits them.

    This is a striking discovery that says maybe polyphenols have reached their upper limits.  This is sure to catch the dietary supplement industry off guard.  But just how to put a limit on these molecules found in coffee, tea, wine, citrus juices and dietary supplements?

    In over a decade spent counseling dietary supplement users on the telephone, many times I have heard callers say they couldn’t continue taking a newly added dietary supplement because it caused heart palpitations.  Another common report is insomnia when taking herbal supplements.

    It has become clear that polyphenols go from promoting mental focus and alertness at low dose to anxiety and even panic attacks at high dose as stress hormone levels rise.

    Even more troubling is research conducted by Paul J. Fitzgerald who links a wide range of diseases, including macular degeneration, lupus, heart flutters (atrial fibrillation) and metabolic syndrome to elevated levels of adrenal hormones.  Ken Eagles links elevated levels of stress hormones to sudden cardiac death.  Yikes!

    Few would argue that stress plays a strong role in disease.  Maybe the precise pathway in which stress operates to worsen disease is just now being uncovered.  Stress hormones are elevated by life’s challenges to survival, not by dietary supplements.  But strikingly, overuse of promising natural remedies from herbs and spices may inhibit the enzyme that keeps a lid on stress hormones associated with these very diseases.

    The right dose

    The question arises, just what would be the optimal dose of polyphenols to produce beneficial health effects without over-inhibition of a stress-limiting enzyme?

    One study shows the intake of polyphenols in beverages alone (wine, tea, coffee, juice) amount to about 180 milligrams per person per day (in Spain).  Yet another report says the intake of polyphenolic molecules from the diet could be as much as 1 gram (1000 milligrams) per day.  So the typical diet is fairly rich in polyphenols already.  Concentrated polyphenolic dietary supplements may elevate intake levels into an undesirable range.

    Studies involving wine demonstrate that consumption of 3-to-5 (5-oz) glasses of dark, aged red wine produced the lowest heart disease mortality rate.  Beyond 5 glasses a day increased coronary artery disease mortality rates.  Given that dark, aged red wine provides about 60 milligrams of wine solids known as polyphenols (resveratrol, quercetin, catechin, kaempferol, malvidin, gallic acid, ferulic acid) per glass, that amount of red wine would provide ~180-to-300 milligrams of these antioxidant molecules.

    An animal study where a combination of polyphenols was used showed that the human equivalent of 100-350 milligrams of polyphenols (quercetin, resveratrol, ferulic acid) reduced damage to the rodent heart while ten-times that dose (1750 mg) increased damage in an experimental heart attack model.

    These studies suggest the optimal intake range for polyphenol supplements may be in the range of 100-350 milligrams.

    The precise polyphenol content of foods and beverages can be accessed online at Polyphenol-Explorer.  A briefer online tool can be accessed here.

    Herbal stress relievers to the rescue

    Modern medicine’s answer to out of control stress hormones is to prescribe adrenal hormone blockers (known as beta blockers).  Paul Fitzgerald notes that users of beta-blockers have lower rates of cancer and Alzheimer’s disease.

    Of course nature has its own anti-stress agents in a class of herbals known as adaptogens (bacopa, ginseng, rhodiola and ashwaganda), as all inhibit stress hormones.  Generally, adaptogens require large doses to work, in excess of 1000 milligrams.

    Nature’s “beta blocker” is L-theanine, an extract from green tea.  In doses ranging from 100-400 milligrams it has been found to produce noticeable reduction in stress hormone levels.  Near-pure L-theanine is available in dietary supplements.

    Of course, over-dosing on polyphenol dietary supplements and then trying to counter any adverse effects with adaptogens or theanine would be akin to playing with fire and continually relying on fire extinguishers.

    It is not uncommon these days to find elite supplement users have a bottle of curcumin, resveratrol, milk thistle, green tea, cinnamon and grape seed extracts on their kitchen table.  Polyphenol enthusiasts may be wise to limit dosage.

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