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NEWSLETTER 10 : Brain function - The Effects of Pharmaceuticals and Nutraceuticals on Brain
                           (Updated November 2002)

Pharmaceuticals
Nutraceuticals
Categories of Nutraceuticals
Nutraceuticals and Brain Function
Choice of the Nutraceuticals
Conclusion

Pharmaceuticals

Pharmaceuticals influence metabolic processes, precipitating or slowing down the pace of biochemical reactions.

Most pharmaceuticals do so without becoming part of the metabolic process they influence.

Pharmaceuticals are synthetic molecules, strangers to our metabolism. As a rule, most pharmaceuticals have potent side effects.

The Physician Desk Reference lists more than 150 different pharmaceuticals to influence brain function.

The Physician Desk Reference also describes extensively the adverse reactions induced by the products, the contraindications and the precautions for use.

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Nutraceuticals

Stephen DeFelice, M.D., chairman of the Foundation for Innovation in Medicine (FIM) , is credited with coining the term nutraceuticals.

His definition encompasses foods with a health benefit, medical foods, and dietary supplements, including herbals.

The American Nutraceutical Association (ANA) expands the definition :

Nutraceuticals are functional foods that have potentially disease-preventing and health-promoting properties. They are also naturally occurring dietary substances in pharmaceutical dosage forms, thus including dietary supplements as defined by the DietaryĘSupplement Health & Education Act of 1994 (DSHEA), as well as comparable substances unintended for oral ingestion, such as creams and lotions. Covered under DSHEA are nutritional products such as vitamins, minerals, medicinal herbs, and metabolic factors (such as CoQ10 and alpha lipoic acid).

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Categories of Nutraceuticals

Nutraceuticals also influence metabolic processes.

A first category of nutraceuticals acts like pharmaceuticals. They influence metabolic processes without becoming part of it. The big difference between pharmaceuticals and nutraceuticals acting like pharmaceuticals is that nutraceuticals induce less side effects and are better tolerated than pharmaceuticals.

A second category of nutraceuticals act differently, becoming part of the metabolic process they influence.

Models for the first category are elaborated plant derived substances: Examples are the active molecules of Siberian ginseng, Ginkgo biloba, psyllium, lycopene, Pygeum africanum, and St John's wort.

Models for the second category are: Amino acids (like arginine, carnitine), all vitamins and minerals, and the omega-3 essential fatty acid Docosahexaenoic acid (DHA).

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Nutraceuticals and Brain Function

Some nutraceuticals influence brain function. Examples are: Kava Kava, Ginkgo Biloba, and St John's Wort.

In Germany physicians prescribe St John's Wort for depression seven times more than pharmaceuticals.

The August 3, 1996 issue of the British Medical Journal (BMJ) contains an analysis of approximately 25 such studies that suggest that St. John's Wort is better than a placebo, and that it is just as helpful as commonly used drugs, with less side effects such as headaches or vomiting.

However, several adverse effects have been reported in association with the usage of St. John's Wort, including:

gastrointestinal discomfort, such as upset stomach
allergic reactions
fatigue
restlessness
increased sensitivity to sunlight (use a sunscreen or sunblock while on St. John's Wort)
dry mouth
confusion
dizziness

Components of St. John's Wort may also cause an increase in blood pressure, which could result in a stroke.

Whether a St. John´s Wort product is more or less effective may also rest on how the product is made.

Different methods produce different combinations of the basic ingredients. Furthermore, the origin of the plant and the cultivation method determine the content of its active ingredients.

In Germany the drug is made with an alcohol extraction method. In the United States the drug is often made using a water extraction method, which may produce a product with a different activity.

In an independent test commissioned by the Los Angeles Times, three of 10 brands of St. John's wort had no more than about half the potency listed on the label. Four other brands had less than 90 percent of the potency listed. One of the lowest-scoring products sampled, with about 20 percent of the labeled potency, was from Sundown Herbals, a division of Rexall, the nation's No. 1 distributor of dietary supplements.

Read more about St John's Wort in a web page of the Columbia University.

A better alternative to pharmaceuticals and to nutraceuticals with side effects is to restore a dysrupted brain function with an adequate minerals and vitamins supplementation.

The rational behind this is that mineral deficiency is an overall reality and that mineral deficiency triggers several brain dysfunctions.

Selenium and lithium are two minerals essential for brain function.

Selenium

A selenium deficiency plays a special role in brain.

Persons with low selenium status experience relatively depressed moods.

Hawkes, Wayne Chris; Hornbostel, Linda. Effects of dietary selenium on mood in healthy men living in a metabolic research unit. Biological Psychiatry, 1996 Jan, v39 (n2):121-128.

Nine surveys conducted between 1980 and l963 indicate a continuing negative relationship between selenium levels in fodder crops and US schizophrenia (SZ) prevalence. Wich is to say that the disease is more prevalent in parts of the country where the soil and water content of selenium is lower.

International similarities in the spatial distributions of SZ and celiac disease, cancer of the esophagus, and multiple sclerosis (all of which appear to involve selenium inadequacy as either a cause or an effect) further support a role for selenium deficiency in SZ.

Selenium affects the activity of enzyme systems, either as a component of an enzyme or as the selenium ion. Low glutathione perioxidase levels found in a specified schizophrenic population could be explained by a problem in the biometabolism of selenium.

Brown Jr., James S.; Foster, Harold D. Schizophrenia: An update of the selenium deficiency hypothesis. Journal of Orthomolecular Medicine, 1996, v11 (n4):211-222.

Lithium

Small amounts of lithium help maintain brain function.

(Note: Lithium is extensively used for brain disorders at dosages in the milligram range. We are talking here of lithium in the nutritional range. in the microgram range, which is one thousand times lower)

In a placebo controlled clinical trial it was found that the intake of trace amounts of lithium improves mood, friendliness and energy.

A total of 24 subjects, 16 males and 8 females, average age 29.4 ± 6.5 yr, were randomly divided into two groups. Group A received 400 µg/d of lithium orally, in tablets composed of a naturally lithium-rich brewer's yeast, for 4 wk. Group B was given normal, lithium-free brewer's yeast as a placebo. All the subjects of the study were former drug users (mostly heroin and crystal methamphetamine). Some of the subjects were violent offenders or had a history of domestic violence. The subjects completed weekly self-administered mood test questionnaires, which contained 29 items covering parameters measuring mental and physical activity, the ability to think and work, the mood condition, and the level of emotionality. In the lithium group, the total mood test scores increased steadily and significantly during the period of supplementation. The 29 items were furthermore placed into three subcategories reflecting happiness, friendliness, energy and their negative counterparts. In Group A the scores increased consistently for all subcategories until wk 4 and remained essentially the same in wk 5. In Group B, the combined mood test scores showed no consistent changes during the same period. The only positive change in some members of Group B occurred during Wk 1 and was attributed to a placebo effect. In Group B, the placebo effect was noticeable for the subcategories of energy and friendliness; the happiness scores showed no surge and declined during the entire period of observation. Based on these results and the analysis of voluntary written comments of study participants, it is concluded that lithium at the dosages chosen had a mood-improving and -stabilizing effect.

G.N. Schrauzer and E. Devroey. Effects of Lithium Supplementation on Mood. Biological Trace Element Research vol 40, 1994. pp 89-101.

Vitamins of the B group

Folate Studies of depressed patients show that many are deficient in folates.

The authors examined the relationships between levels of three metabolites (folate, vitamin B12, and homocysteine) and both depressive subtype and response to fluoxetine treatment in depressed patients.

Overall, the results are consistent with findings linking low folate levels to poorer response to antidepressant treatment. Folate levels might be considered in the evaluation of depressed patients who do not respond to antidepressant treatment.

Fava M; Borus JS; Alpert JE; Nierenberg AA; Rosenbaum JF; Bottiglieri T. Folate, vitamin B12, and homocysteine in major depressive disorder. American Journal of Psychiatry, 1997 Mar, 154(3):426-8.

Vit B12 and folate have a synergic action.

We report the occurrence of hemolysis and red cell fragmentation mimicking microangiopathic hemolytic anemia, malabsorption and folic acid deficiency in the course of vitamin B12 deficiency. Appropriate replacement therapy corrected all abnormalities. An association between hemolysis, malabsorption and folic acid deficiency should lead physicians to search for signs of vitamin B12 deficiency.

Jubault V; De Lacroix-Szmania I; Zittoun J; Jouault H; Lesprit P; Godeau B; Schaeffer A. Hemolysis and schizocytosis, malabsorption and the "folate trap": unusual semiological peculiarities associated with vitamin B12 deficiency Revue de Medecine Interne, 1998 Dec, 19(12):921-3.

Omega-3 Essential Fatty Acids

The omega-3 essential fatty acid Docosahexaenoic acid (DHA) is an important constituent of brain cells' membrane .

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Choice of the Nutraceuticals

Selenium

In the US, selenium is available over the counter in tablets and capsules with dosages varying from 50 to 300 microgram. 250 to 300 microgram per day for an adult is recommended by the experts.

One should prefer products that contain at least 250 microgram of selenium per serving and also contain copper and zinc.

Copper is essential for bloodvessel wall maintenance (Brain bloodvessels included) and zinc for glucose metabolism (Glucose is the fuel for the brain cells).

The addition of vanadium and of chromium to the formula is a plus, since both minerals also help regulate glucose utilization.

Lithium

Lithium is available in plant derived liquid mineral formulas. A typical product contains up to 87 microgram of lithium per serving of one Fl. oz.

In the US, there is no federal Recommended Daily Allowance (RDA) for lithium.

Nevertheless, researchers recommend 100 microgram per day for its mood-improving and -stabilizing effect.

Vitamins of the B group

Vitamins of the B group are available over the counter in a great variety of forms and dosages.

Preferred product should contain more per serving than the RDA's for the vitamins of the B group.

Essential omega-3 fatty acids

Essential omega-3 fatty acids are available in cold ocean fish, in fish oil, and in flax seed and flax seed oil.

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Conclusion

As opposed to some nutraceuticals and to all pharmaceuticals, minerals and vitamins in appropriated dosage are deprived of side effects.

In all cases of brain dysfunction, a supplementation with selenium, lithium, vitamin of the B group and omega-3 essential fatty acids should be the mandatory first step.

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