1. COENZYME Q10

INDICATIONS: Studies have shown either deficiency or benefit of supplementation in cardiovascular disease(1), high blood pressure(2), mitral valve prolapse(3), coronary artery bypass surgery(4), angina(5), congestive heart failure(6) diabetes mellitus(7), periodontal disease(8), immune deficiency(9), cancer(10), assisting weight loss(11), muscular dystrophy(12), and athletic performance enhancement(13). Bioavailability studies reveal the best preparations to be soft-gelatin capsules containing CoQ10 in an oil base(soybean oil). Farmacopia carries the Thorne soybean oil base CoQ10.

DOSAGE: The usual dosage is 50 - 150 mg/day with doses up to 300 mg/day in severe heart disease. Some studies used 2 mg/kg.

SIDE EFFECTS AND INTERACTIONS: No adverse reactions have been reported. Safety during pregnancy and lactation has not been proven. No adverse interaction with any drug or nutrient has been reported although many drugs adversely affect CoQ10 levels and CoQ10 can mitigate some drug side effects, including effects from cholesterol-lowering agents, beta-blockers and psychotropic agents. Of interest is that the congestive heart failure seen with long-term beta-blocker therapy may be related to CoQ10 deficiency. In addition, the cardiac side effects of phenothiazines and tricyclic antidepressants may be related to inhibition of CoQ10 function. This inhibition is reversible by CoQ10 administration.

Coenzyme Q10(CoQ10) is a fat soluble quinone, created from tyrosine, occurring in the mitochondria of all cells. It is a cofactor in the electron transport chain that generates ATP. It also recycles vitamin E. It's level is reduced by HMG-CoA reductase inhibitors and susceptibility to deficiency is greatest in the most metabolically active cells including the heart, gingiva, immune system and gastric mucosa. Inadequate nutritional intake, a genetic or acquired defect in synthesis, increased tissue needs or advancing age can lead to inadequate tissue levels.

Coenzyme Q10 acts as a lipid soluble anti-oxidant, which may protect against atherogenesis. It appears to reduce blood viscosity. Deficient levels have been found in hypertension and other cardiovascular disorders. The mechanism of Coenzyme Q10 benefit is not known in all the disorders mentioned under indications, although an improvement in energy-dependent processes, it's anti-oxidant, anti-atherogenic and immune-enhancing properties are no doubt implicated.

1. Langsjoen H, et al., Usefulness of coenzymeQ10 in clinical cardiology: A long-term study. Mol. Aspects Med 15(Suppl.),S165-S175, 1994
2. Digiesi V, et al., Coenzyme Q10 is essential hypertension. Mol Aspects Med 15 (Suppl.), S257-S263, 1994
3. Oda T and Hamamoto K, Effect of coenzyme Q10 on the stress-induced decrease of cardiac performance in pediatric patients with mitral valve prolapse. Jap Circ J 48, 1387, 1984
4. Chello M, et al., Protection of coenzyme Q10 from myocardial reperfusion injury during coronary artery bypass grafting. Ann Thorac Surg 58, 1427-1432, 1994
5. Kamikawa T, et al., Effects of coenzyme Q10 on exercise tolerance in chronic stable angina pectoris. Am J Cardio 56, 247, 1985
6. Baggio E, et al., Italian multicenter study on the safety and efficacy of coenzyme Q10 as adjunctive therapy in heart failure. CoQ10 Drug Surveillance Investigators. Mol Aspects Med 15(Suppl.), S287-S294, 1994
7. Kishi T, et al., Bioenergetics in clinical medicine, XI, Studies on coenzyme Q10 and diabetes mellitus. J Med 7, 307, 1976
8. Hanioka T, et al., Effect of topical application of coenzyme Q10 on adult periodontitis. Mol Aspects Med 15(Suppl.), S241-S248, 1994
9. Folkers K, et al., Increase in levels of IgG in serum of patients treated with coenzyme Q10. Res Commun Chem Pathol Pharmacol 38, 335, 1982
10. Lockwood K, Moesgaard S, and Folkers K, Partial and complete regression of breast cancer in patients in relation to dosage of coenzyme Q10. Biochem Biophys Res Comm 199, 1504-1508, 1994
11. van Gaal L, de Leeuw ID, Vadhanavikit S, and Folkers K, Exploratory study of coenzyme Q10 in obesity. In: Biomedical and Clinical Aspects of Coenzyme Q, Vol. 4. Folkers K and Yamamura Y (eds.). Elsevier Science Publ., Amsterdam, 1984, pp. 369-373
12. Folkers K and Simonsen R, Two successful double-blind trials with coenzyme Q10(vitamin Q10) on muscular dystrophies and neurogenic atrophies. Biochem Biophys Acta 1271, 281-286, 1995
13. Vanfraechem JHP and Folkers K, Coenzyme Q10 and physical performance, In: Biomedical and Clinical Aspects of Coenzyme Q10(see above), pp.235-241

2. DHEA

INDICATIONS: Recent experimental studies have shown a role and possible benefit of supplementation of DHEA in a number of conditions including diabetes(1), heart disease(2), cancer(3), autoimmune diseases(4), AIDS(5), aging(6), osteoporosis(7), rheumatoid arthritis(8) and hereditary angioedema(9).

DOSAGE: Proper usage of DHEA should be preceded by a DHEA Sulfate blood level test. Dosages have ranged from 50 mg to 2500 mg/day. The goal is achieving blood levels seen in younger individuals. Men should probably have a PSA level and rectal exam, and the hormone should be avoided if prostate cancer is present. Women should have serum estradiol and progesterone levels measured as well as having a PAP test.

SIDE EFFECTS AND INTERACTIONS: Side effects in men include increasing masculinity and libido. In women, side effects include hirsutism, uterine bleeding. Dehydroepiandrosterone(DHEA) is the principle steroid hormone secreted by the adrenal glands with circulating levels of DHEA and its ester DHEA-sulfate 20 times higher than any other adrenal hormone. It has been assumed up, until recently, that it served only as a buffer hormone for the production of other hormones, including estrogen and testosterone. DHEA levels decline dramatically with age, unlike any other adrenal hormone, in both men and women. It may play a role in the body's ability to repair itself, to build muscle and maintain strength, lean body mass and natural immunity.

1. Loviselli A, Pisanu P, Cossu E, et al., Low levels of Dehydroepiandrosterone sulfate in adult males with insulin-dependent diabetes mellitus. Minerva Endocrinol 1994; 19: 113-119
2. Barrett-Conner E, Knaw K-T, Yen S.S.C. A prospective study of Dehydroepiandrosterone sulfate, mortality, and cardiovascular disease. N Engl J Med 1986; 316; 1519-1524
3. Gordon GB, Shantz LM and Talalay P. Modulation of growth, differentiation and carcinogenesis by DHEA. Advances in Enzyme Regulation 26:355-383, 1987
4. Van Vollenhoven RF, Engleman EG, McGuire JL. An open study of dehydroepiandrosterone in systemic lupus erythematosis. Arthritis Rheum 1994;37:1305-1310
5. Jacobson MA, Fusaro Re, Galmarini M, Lang W. Decrease serum dehydroepiandrosterone is associated with an increased progression of human immunodeficiency virus infection in men with CD4 cell counts of 200-499. J Infect Dis 1991; 164: 864-868
6. Morales AJ, Nolan JJ, Nelson JC, Yen SS. Effects of replacement dose of dehydroepiandrosterone in men and women of advancing age. J Clin Endocrinol Metab 1994; 78: 1360-1367
7. Devogelaer, J.P., J. Crabbe, and C.N. De Deuxchaisnes. Bone mineral density in Addison's disease: Evidence for an effect of adrenal androgens on bone mass, Br Med J 1987; 294: 798-800
8. Sambrook, P.N., et al. Sex hormone status and osteoporosis in postmenopausal women with rheumatoid arthritis. 1988; Arthritis Rheum 31:973-978
   1. Koo E, Feher KG, Feher T, Fust G. Effect of dehydroepiandrosterone on hereditary angioedema. Klin Wochenschr 1983; 61: 715-717

3. FIBER SUPPLEMENTS

INDICATIONS: Studies show benefit in irritable bowel syndrome(1), hypercholesterolemia(2), obesity(3,4), and constipation.

DOSAGE: Start with 1 -2gm before meals and at bedtime, gradually increasing each dosage to 5 gm.

SIDE EFFECTS AND INTERACTIONS: Fiber in pill form is contraindicated in esophageal disorders. Drink plenty of water when taking fiber supplements. Large amounts of fiber may cause impaired absorption of some minerals. Fiber can also inhibit the absorption of certain drugs, so the fiber should not be ingested around the time of drug ingestion.

Dietary fiber is divided into soluble fiber such as hemicelluloses, mucilages, gums, lignan precursors and pectins, and insoluble fibers like wheat bran. Fiber promotes regular bowel movements by increasing the weight and water content of stool, encourages advantageous intestinal microflora by lowering the gut pH and fermentation of insoluble fiber provides short-chain fatty acids, fuel for colonic mucosal cells. Soluble fibers lower cholesterol by forming a gel that binds cholesterol and bile acids in the gut. Lignans have additional anti-cancer, antibacterial, antifungal and antiviral properties. There is extensive epidemiologic evidence that a diet low in fiber results in chronic degenerative disorders including osteoarthritis, rheumatoid arthritis, gout, heart disease and cancer . The best sources for water-soluble, non-laxative fiber is psyllium, guar gum, glucomannan, gum karaya and pectin.

1. Spiller GA, Dietary Fiber in Health and Nutrition. CRC Press, Boca Raton, FL, 1994
2. Glore SR, et al., Soluble fiber and serum lipids: A literature review. J Am Diet Assoc. 94, 425-436. 1994
3. Krotkiewski M, Effect of guar gum on body weight, hunger ratings and metabolism in obese subjects. Clinical Science 66, 329-336, 1984
4. Rossner S, et al., Weight reduction with dietary fiber supplements: Results of two double-blind studies. Acta Med Scand 222, 83-88, 1987

4. GLUCOSAMINE SULFATE

INDICATIONS: The principle use of GS is in osteoarthritis with one study showing accelerated healing in patellar sports injuries(1) Numerous studies have shown better results with GS than NSAIDS in osteoarthritis (2,3). In addition, NSAIDS can inhibit cartilage repair and accelerate cartilage destruction thereby slowly worsening the osteoarthritis. It should be added that cartilage extracts, shark cartilage, chondroitin sulfate, green-lipped mussels and sea cucumber products are large molecules and difficult to absorb. There are apparently no significant supportive clinical studies utilizing the oral form of these products.

DOSAGE: The standard dosage of GS is 500 mg three times per day. Obese individuals may need higher dosages calculated as 20mg/kg.

SIDE EFFECTS AND INTERACTIONS: Side effects are uncommon and can include stomach upset, heartburn, diarrhea, nausea and indigestion. If symptoms occur, try taking GS with meals. No allergic reactions have been reported. Allergy to sulfa drugs or sulfite does not equate to an allergy to sulfate, which is a significant constituent of blood. To stabilize the glucosamine sulfate formative reaction, some manufacturers add large amounts of sodium, which can add unwanted sodium to the diet. The Thorne product has a balanced mixture of sodium(20 mg/capsule) and potassium(32 mg/capsule) to avoid this problem.

Glucosamine is a simple aminomonosaccharide produced in the body by the combination of glucose and glutamine. It is found in many tissues and secretions and is the primary substrate for the synthesis of proteoglycans such as chondroitin sulfate and hyaluronic acid which, in turn, give rise to collagen and form the ground substance of articular cartilage. Glucosamine also inhibits the degradation of proteoglycans. These factors explain it's positive influence on osteoarthritis. Proteoglycans hold water, giving connective tissue flexibility and resilience. Sulfur is an essential nutrient for joint tissue where it helps stabilize the connective tissue matrix of cartilage, tendons and ligaments. For this reason, the sulfur portion of glucosamine sulfate(GS) is important, making glucosamine sulfate the preferred supplement compared to glucosamine hydrochloride or N-acetyl-glucosamine. GS is also a component of glycoproteins and glycosaminoglycans, which are essential components of cell membranes and cell surface proteins as well as interstitial structural molecules that hold cells together. GS plays a role in the formation of articular surfaces, tendons, ligaments, synovial fluid, skin, bone, nails, heart valves, blood vessels, and in mucous secretions of the digestive, respiratory and urinary tracts.

GS is a small molecule. soluble in water, and well absorbed in the small intestine. N-acetyl-glucosamine is quickly digested by intestinal bacteria or altered by intestinal cells and may not be absorbed by an oral route.

1. Bohmer D et al. Treatment of chondropathiua patellae in young athletes with glucosamine sulfate, in N Bachl, L Prokop, R Sucher, Eds. Current Topics in Sports Medicine. Proc World Congress of Sports Med. Vienna. 1982. Urban and Schwarzenberg, 1984
2. Vaz AL, Double-blind clinical evaluation of the relative efficacy of ibuprofen and glucosamine sulfate in the management of osteoarthritis of the knee in out-patients. Curr Med Res Opin 8, 145-149, 1982
   1. D'Ambrosia ED et al., Glucosamine sulfate: A controlled clinical investigation in arthritis. Pharmatherapeutica 2, 504-508, 1982

5. ALPHA-LIPOIC ACID

INDICATIONS: Lipoic acid has shown benefit in diabetic neuropathy(1) and in AIDS(2).

DOSAGE: Dosage is time released. 300 to 600 mg/day.

SIDE EFFECTS AND INTERACTIONS: There are no reported side effects. It may spare vitamin C and E and other anti-oxidants. Oxidative decarboxylation of pyruvate involves an enzyme complex of lipoic acid with thiamine and niacin so that lipoic acid works synergistically with these other vitamins. It may improve sugar control in diabetes thus allowing a reduction in insulin or oral hypoglycemic agents. Glucose levels should be monitored.

Alpha-lipoic acid is composed of an 8 carbon fatty acid chain and two sulfur molecules and acts in a reduced form, dihydrolipoic acid(DHLA) in the body after absorption. It has the unique property of being antioxidant in the water and fat soluble domains. It regenerates reduced glutathione and ascorbic acid and may have an indirect impact on recycling vitamin E. As lipoamide, it functions as a cofactor in oxidative decarboxylation of pyruvate, an important metabolic step in energy production. It is also involved in the oxidative decarboxylation of alpha-ketoglutarate and branched chain keto acids. Both lipoic acid and DHLA have metal chelating activity against cadmium, manganese, copper, zinc, iron and mercury. Its benefit in diabetic neuropathy relates to its antioxidant effect along with an improvement in blood sugar metabolism, reduced glycosylation of proteins, improved blood flow to peripheral nerves and stimulation of nerve regeneration(3). Supplementation may improve energy metabolism, especially in individuals with reduced levels, including those with diabetes, liver cirrhosis and heart disease.

1. Packer L, Antioxidant properties of lipoic acid and its therapeutic effects in prevention of diabetes complications and cataracts. Annals NY AcadSci 738, 257-264, 1994.
2. Fuchs J, et al., Studies on lipoate effects on blood redox state in human immunodeficiency virus infected patients. Arzneim Forsch 43, 1359-1362, 1993
3. Nagamatsu M, et al., Lipoic acid improves nerve blood flow, reduces oxidative stress, and improves distal nerve conduction in experimental diabetic neuropathy. Diabetes Care 18, 1160-1167, 1995

6. MEDIUM CHAIN TRIGLYCERIDES

INDICATIONS: Weight loss(1); For almost 50 years, MCTs have also been used in malabsorption syndromes of diverse etiology(2). Finally, they can be used in the ketogenic diet for epilepsy under physician supervision(3).

DOSAGE: Dosage for weight loss is 1 to 2 tablespoons/day. Other application require physician supervision.

SIDE EFFECTS AND INTERACTIONS: MCTs do not have adverse effects although diabetics and individuals with liver disease require physician supervision because of the possibility of acidosis with them. MCTs do not interact with any nutrient or drug.

Medium chain triglycerides(MCTs) are 6 to 12 carbon length fatty acids esterified to glycerol.. Unlike the long chain triglycerides (LCTs - 14 to 24 carbons in length) which are the storage form for body fat, MCTs are rapidly oxidized in liver mitochondria. The same calorie meal with MCTs has three times the thermogenic effects as the meal with LCTs resulting in weight loss. This explains its use in weight loss. In addition , MCTs do not raise the blood lipid levels. They are absorbed without pancreatic enzymes or bile acids explaining their use in malabsorption syndrome.

1. Hill JO, et al., Thermogenesis in man during overfeeding with medium chain triglycerides. Metabolism 38, 641-648, 1989
2. Bach AC and Babayan VK, Medium chain triglycerides. An update. Am J Clin Nutr 36, 950-962, 1982
3. Signore, Ketogenic diet with medium chain triglycerides. J Am Diet Assoc. 62, 285-290. 1973

7. MELATONIN

INDICATIONS: Melatonin supplementation is beneficial in jet-lag(1), insomnia(2) and cancer(3). Data in depression is conflicting.

DOSAGE: Precise dosing is unknown although dosages as low as 0.1 mg can be sedating if melatonin secretion is deficient. The 24 hour urinary excretion of melatonin is 0.03 mg suggesting that the standard dose of 3 mg is more than enough.

SIDE EFFECTS AND INTERACTIONS: Daytime dosing may cause depression. Vitamin B12 appears to increase melatonin secretion accounting for the improvement in sleep-wake disorders with vitamin B12 supplementation.

Melatonin(N-acetyl-5-methoxytryptamine) is produced from tryptophan and is controlled by exposure to cycles of light and dark. Production is stimulated by darkness by way of a multi-synaptic neural pathway connecting the pineal gland to the external environment via the retina. It has high nocturnal levels and levels are reduced by exposure to light as well as electromagnetic fields associated with video monitors, microwave ovens and electrical wires. Some individuals are deficient in pineal melatonin secretion, and levels decrease with age. Melatonin may play a central role in circadian hormone regulation, which can be disrupted in jet-lag, night shift work, blindness and seasonal dark-light cycle changes. Its use in insomnia relates to its role in controlling sleep-wake cycles. Melatonin exerts anti-oxidant effects. It appears to inhibit both the initiation and promotion of certain cancers, and may aid the anti-cancer effects of other agents.

1. Lino A, et al., Melatonin and jet lag: Treatment schedule. Biol Psychiatry 34, 587, 1993
2. Zhdanova IV, et al., Sleep-inducing effects of low doses of melatonin ingested in the evening. Clin Pharmacol Ther 57, 552-558, 1995
3. Lissone P, et al., A randomized study with subcutaneous low-dose interleukin 2 alone vs. interleukin 2 plus the pineal neurohormone melatonin in advanced solid neoplasms other than renal cancer and melanoma. Br J Cancer 69, 196-199, 1994

8. PHOSPHATIDYL SERINE

INDICATIONS: Double blind studies have shown benefit in dementia(1) and depression(2) in the elderly.

DOSAGE: The standard dosage is 100 mg three times a day.

SIDE EFFECTS AND INTERACTIONS: No side effects or adverse interactions have been reported.

Phosphatidylserine(PS) is the major acidic phospholipid in the brain occurring in cell membranes. PS enhances membrane fluidity. Aging is associated with altered neuronal membrane lipid composition, enzymatic activity, decreased neurotransmitter synthesis and metabolism and decreased synaptic activity. PS appears to reverse some of these changes and also helps re-establish the normal down-regulation of cortisol secretion that is increased in chronically stressed individuals. PS crosses the blood-brain barrier with an affinity for the hypothalamus. Of interest is that supplementation does not increase monoamine neurotransmitter levels. It's benefit in dementia and depression may relate to improved brain cell membrane fluidity.

Thorne's lecithin based PS is the only commercially available pre-formed vegetarian PS product(not just a calcium-magnesium chelate of serine).

1. Cenacchi T, et al., Cognitive decline in the elderly: A double-blind, placebo-controlled multicenter study on efficacy of phosphatidylserine administration. Aging 5, 123-133, 1993
2. Maggioni M, et al., Effects of phosphatidylserine therapy in geriatric patients with depressive disorders. Acta Psychiatr Scand 81, 265-270, 1990

9. PREGNENOLONE

INDICATIONS: Pregnenolone in animals improves their memory(1) and there are studies in progress using it in Alzheimer's Disease. Low levels correlate with depression(2) and supplementation increases deep, slow wave, sleep(3). It has shown benefit in spinal cord injury(4), and modest benefit in multiple sclerosis(5). It may have a positive modulating effect on the immune system and work is being done on its possible use in hormone replacement therapy.

SIDE EFFECTS AND INTERACTIONS: There are no long term studies to evaluate safety. Laboratory animals have not shown any side effects and human trials caused one isolated case of skin rash. There is a theoretical potential for hypertension with its use. Medical supervision for long term treatment is advised.

Pregnenolone, an adrenocortical hormone, is synthesized from cholesterol and is a precursor to all of the adrenocorticcal hormones including progesterone, DHEA, cortisol, aldosterone, testosterone and estrogen. The transformation of pregnelone depends upon the physiological needs of the body. Its level reduces with age, and some cholesterol lowering drugs can reduce pregnenolone levels. Early research showed that it possessed minor amounts of activity attributed to the other various steroid hormones. There are important links between pregnenolone and DHEA. Early studies showed promise in lupus and rheumatoid arthritis. More studies in humans are needed for this compound which shows promise in a number of disorders and has low toxicity and lack of adverse side effects. Research over the last few decades has waned relative to the early interest in the 1940's and 1950's.

1. Wilkinson, M et. et al., Modulation of cardiac M2 muscarinic receptor binding by progesterone-related steroids. Jour Mol Cell Cardiol,9/27 (9) 1995, 1831-1839
2. George, M et al., CSF neuroactive steroids in affective disorders: pregnenolone, progesterone and DBI. Biol Psch, 35(10), 1994 775-780
3. Steiger A, et al., Neurosteroid pregnenolone induces sleep-EEG changes in man compatible with inverse agonistic Gaba receptor modulation, Brain Res 615, 1993, 267-274
4. Guth, Lloyd, et al., Key role for pregnenolone in combination therapy that promotes recovery after spinal cord injury. Proceeding of the Nat Acad of Sci of USA, Dec6, 1994, v91, n25, 12308-12
5. Sahelian, Ray Pregnenolone, A Practical Guide, Marina Del Ray, Calif., Melatonin/DHEA Research Institute, 1996

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