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Cholesterol Lowering Natural Alternatives (Doctors' Edition) PDF Print E-mail
Written by Dr. Edward Zimmer   

One area demanding major attention in daily medical practice is that of controlling blood lipoprotein levels. Situations commonly occur where the need for alternatives to prescriptions have to be considered. These include times when a patient has adverse reactions to a drug or refuses to take a prescription for some reason. Physicians should have alternative options to suggest for patients that offer some support in the literature as being effective and safe. This issue will detail a few of the cholesterol lowering natural alternatives that have decent support for their use in modifying blood lipid levels.

Cholesterol Lowering Natural Alternatives

Niacin (Nicotinic Acid)

  • Most health professionals are familiar with the beneficial effects that niacin has on lipid profiles. Niacin has been shown to decrease triglycerides between 20-50%, decrease LDL-C between 5-25%, decrease Lp(a) between 15-25%, and increase HDL-C 15-35%.1,2
  • A major concern raised regarding the use of non-prescription niacin is whether the label claim for the OTC vitamin is accurate to the amount of niacin actually found in the tablets. This concern is rightfully raised due to the lack of federal regulation on nutritional supplements. Meyers, et al investigated this question by purchasing various OTC preparations from health food stores, pharmacies, and internet companies.3 500 mg tablets/capsules were quantified by HPLC. The average free nicotinic acid for immediate release preparations was 502.6 mg and for sustained-released was 520.4 mg. Thus, OTC preparations did contain accurate amounts of niacin.
  • Another concern with niacin use is the side-effect of flushing. This effect is reduced with extended release (Niaspan) and sustained release preparations. Flushing can also be reduced by titrating the dose of niacin up to 1.5 g/day over a 2 week period of time, by administering the dose with food, and by increasing water intake with the dose.4
  • Niacin’s lipid-regulating actions are likely due to its effect on lipoprotein metabolism. One key action is the inhibition of free fatty acid mobilization from peripheral adipose tissue to the liver. Thus, a decrease in hepatic synthesis of triglycerides, VLDL, and LDL are reduced.5 Niacin also appears to reduce the breakdown of apo A-1 which could account for the increased production of HDL.6 Long-term niacin therapy has been shown to lower CVD and total mortality.7
  • What about using other forms of niacin (niacinamide or inositol hexanicotinate) for lipid control? Niacinamide is NOT an effective lipid-altering agent. The jury is still out on the so-called “flush-free” inositol hexanicotinate. The data is limited at this time. There is an ongoing randomized, double-blind, controlled trial being conducted at the University of Minnesota Medical School comparing inositol hexanicotinate to sustained-released niacin. I will inform you of the results of this study when they become available. Until then, I currently do not recommend the use of this form of niacin for lipid control.
  • My recommendation for niacin is if the patient has prescription coverage use Niaspan. If not, OTC niacin is way cheaper! There is little good evidence that I have seen to support the claim that OTC niacin will not be effective.

Policosanol

  • Policosanol contains a mixture of open-chained alcohols derived, typically, from purified cane sugar. Policosanol consists mainly of octacosanol (CH3-CH2(26)-CH2-OH).9 It seems that policosanol decreases the synthesis and increases the degradation of HMG-CoA reductase whereas, statins act as competitive inhibitors of this enzyme.10 Also, policosanol has demonstrated improvement in LDL metabolism by increasing LDL binding, uptake, and degradation in human fibroblasts.11 Additionally, policosanol appears to have other cardiovascular benefits including prevention of LDL-C oxidation, reduced platelet aggregation, decreased foam cell formation, and decreased smooth muscle proliferation.
  • A recent prevention study demonstrated that policosanol reduced all mortality and all cardiovascular, coronary, cerebrovascular, and vascular serious adverse events in older patients.8 Policosanol has been studied against popular statin drugs including simvastatin,12,13 pravastatin,14 lovastatin,15,16 and atorvastatin.17 Policosanol at 10 mg/day improved HDL-C to a greater degree and with a better safety profile than did lovastatin. After 12 weeks, policosanol improved LDL-C, total cholesterol, and the LDL-C:HDL-C ratio similar to lovastatin.15

cholesterolMD
  • Dosing of policosanol should be between 10-20 mg/day in divided doses. There is some evidence that there is little additional benefit seen at doses above 20 mg for improvement in lipid profiles. At present the only drug-interaction to consider would be for patients on anticoagulant therapies.

Plant Sterols (Phytosterols)

  • Plant sterols are fats found in fruits and vegetables that have a structure very similar to cholesterol. Their use has been almost exclusively as a food additive in margarine, orange juice, and salad dressings to name a few. The FDA permits the following claim for plant sterols as a food additive:

    “Foods containing at least 0.65 grams per serving of plant sterol esters, eaten twice a day with meals for a daily total intake of at least 1.3 grams, as part of a diet low in saturated fat and cholesterol, may reduce the risk of heart disease.”

  • Sterols inhibit the absorption of cholesterol from the intestinal tract by binding and co-precipitating with cholesterol. This includes both ingested cholesterol and cholesterol excreted in the bile. Additionally, sterols are taken up by the enterocytes that also transport cholesterol and become substrates for ACAT (acyl coenzyme A: cholesterol acyltransferase). Sterols block the esterfication of cholesterol by this enzyme and the unesterfied molecule is then transported back into the lumen and excreted in the feces.18
  • A study published in 2006 showed a statistically significant reduction of Total Cholesterol from 7—11% and LDL-C from 10—15%.19 Triglycerides and HDL-C were not effected. Another recent study of diabetic patients showed a reduction in LDL-C of 26.8%. Non-diabetic participants in this study had LDL-C reductions of 15.1%.20 This suggests that plant sterols may be even more advantageous for us in hypercholesterolemic diabetic patients.
  • The recommended dose of plant sterols is between 2-3 grams a day in divided doses. It is best taken with meals.

Red Yeast Rice

  • Red Yeast Rice is a product which results from the fermentation of rice with red yeast. The discovery of monocolins from RYR led to the development of Monacolin K, lovastatin. RYR also contains 8 other monacolins, sterols, isoflavones, and monounsaturated fats.
  • The question with RYR is whether it simply acts as a statin. Studies using RYR have calculated the daily Monacolin K content of the supplement used as 4.8 mg. This is much lower than dosages used to test lovastatin (20—40 mg). Thus, it is unlikely that the cholesterol lowering effects are due solely to the Monacolin K levels. A yet to be identified synergy amongst the other components found in RYR most likely accounts for its cholesterol lowering effects.
  • Clinically, I have had a number of patients significantly lower their Total Cholesterol and LDL-C using RYR. Human clinical trails using RYR resulted in reduced LDL-C (20-30%), reduced TG (13-30%) and increased HDL-C (15-30%).21,22 Some trials did not show an increase in HDL-C. Other recent studies have suggested that RYR may impart other beneficial effects like lowering hs-CRP, reducing Lp(a), and improving endothelial dysfunction.
  • There is a major problem with RYR preparations typically found in health food stores and on the internet. The benefits seen from using RYR are dependent on the presence of the different monacolin factions. MANY preparations lack significant levels of these important molecules. The total monacolin content of nine different commercially available RYR preparations was evalutated by HPLC and revealed that a number had ZERO monacolin content. 23
  • Thus, I suggest that you tell your patients that buying RYR is like playing a game of chance. The safety profile is very good so that is not a real concern. Thorne Research has a good RYR product which can be found on www.ZimmerNutrition.com. The dose of RYR is between 1-2 grams/day.

Fish Oils

  • The role of omega-3 fatty acids from fish oil in preventing cardiovascular events is well established. Concerning lipoprotein markers, the reduction of serum triglycerides is by far the most significant and consistent clinical response to fish oil ingestion. A meta-analysis of 65 published reports showed TG reduction averaging 25% with fish oil consumption.24
  • The dose for fish oils is important. Most preparations contain only 180 EPA/120 DHA per capsule. These provide a total content of only 300 mg of EPA/DHA. The recommended dose is between 1.5g to 4 g/day. Thus, a patient should be taking a minimum of 5 capsules a day. Most patients take way below this dosage. Informing a patient of proper dosage is important and should not be overlooked.

Pantethine (NOT Pantothenic Acid)

  • Pantethine (Vitamin B5 precursor) can be metabolized to either pantothenic acid (B5) which has no known lipid-altering effects or Cysteamine which does have lipid-altering effects. Thus, a patient should be told to take Pantethine but not Pantothenic Acid. Consistent reductions of Total Cholesterol (10-15%), LDL-C (10-15%), TG (15-20%), and increased HDL-C (15-20%) have been shown. A recent study confirmed the results of previous pantethine studies and also showed an increase in LDL particle size.25
  • The dosage of Pantethine should be between 600 - 900 mg/day taken in divided doses.

Viscous Soluble Fiber

  • Examples of VSF are psyllium, pectin, glucomannan, beta-glucan, and guar gum. These are found naturally in flax, oats, barley, fruits and legumes. VSF trap and eliminate cholesterol-rich bile salts from the intestines. Additionally, they increase the bacterial production of short chain fatty acids which may inhibit hepatic cholesterol biosynthesis.
  • A recent clinical trial showed that the addition of 15 grams/day of psyllium fiber to 10 mg of simvastatin was similar in lipid-lowering as 20 mg of simvastatin without psyllium.26

Garlic

  • There have been nearly 50 studies conducted to assess the lipid-lowering effects of garlic in humans over the past 40 years. Recent meta-analysis suggest that the best and most controlled trials show garlic preparations are better than placebo in cholesterol reduction, but have only a modest effect.27
  • Garlic has been shown, however, to decrease the oxidation of LDL-C and thus may be a good suggestion for patients who only have the need for minor reductions in cholesterol levels.

  • You can contact Dr. Zimmer with any questions, requests, or responses via email or at 317-813-1998 / toll free 1-888-813-1998

REFERENCES

  1. Alderman JD, Pasternak RC, Sacks FM, et al. Effect of modified, well-tolerated niacin regimen on serum total cholesterol, high density lipoprotein cholesterol and the cholesterol to high density lipoprotein ratio. Am J Cardiol 1989;64(12):725-9.
  2. Keenan JM, Fontaine PL, Wenz JB, et al. Niacin revisited. A randomized, controlled trial of wax-matrix sustained released niacin in hypercholesterolemia. Arch Intern Med 1999;151(7): 1424-32.
  3. Meyers CD, Carr MC, Park S, Brunzell JD. Varying cost and free nicotinic acid content in over-the-counter niacin preparations for dyslipidemia. Ann Intern Med 2003 Dec 16;139(12):996-1002.
  4. Pujalte JM, Liavorce EP, Ylescupidez FR. Double-blind clinical evaluation of oral glucosamine sulphate in the basic treatment of osteoarthrosis. Curr Med Res Opin 1980;7(2):110-14.
  5. Knopp RH. Drug treatment of lipid disorders. N Engl J Med 1999;341(7):498-511.
  6. Capuzzi DM, Morgan JM, Brusco OA. Niacin dosing: relationship to benefits and adverse effects. Curr Atheroscler Rep 2000;2(1)64-71.
  7. Ito MK. Advances in the understanding and management of dyslipidemia: using niacin-based therapies. Am J Health Syst Pharm 2003;60(13 Suppl 2):S15-S21.
  8. Mas R, Castano G, Illnait J, et al. Effects of policosanol on morbidity and mortality of older hypercholesterolemic patients. Am Col.. Cardiol. 39{Suppl}, Abstracts of the XIV World Cong. Cardiol. (Sydney, May 5-9, 2002) Abstract 429B, 2002.
  9. Arruzazabala ML, Noa M, Menendez R, et al. Protective effect of policosanol on atherosclerotic lesions in rabbits with exogenous hypercholesterolemia. Baz J Med Biol Res 2000;33:835-840.
  10. Menendez R, Amor AM, Gonzalez R, et al. Effect of policosanol on the hepatic cholesterol biosynthesis of nomocholesterolemic rats. Biol Res 1996;29:253-257.
  11. Menendez R, Fernendez SI, Del Rio A, et al. Policosanol inhibits cholesterol biosynthesis and enhances low density lipoprotein processing in cultured human fibroblasts. Biol Res 1994;27:199-203.
  12. Illnait J, Castano G, Mas R, et al. A comparative study on the efficacy and tolerability of policosanol and simvastatin for treating type II hypercholesterolemia. Can J Cardiol 1997;13:342B.
  13. Ortensi G, Gladstein J, et al. A comparative study of policosanol versus simvastatin in elderly patients with hypercholesterolemia. Curr Ther Res Clin Exp 1997;58:390-401.
  14. Castano G, Mas R, Arruzazabala ML, et al. Effects of policosanol and pravastatin on lipid profile, platelet aggragation and endothelemia in older hypercholesterolemic patients. Int J Clin Pharmacol Res 1999;19(4):105-16.
  15. Castano G, Menendez R, et al. Effects of policosanol and lovastatin on lipid profile and lipid peroxidation in patients with dyslipidemia associated with type 2 diabetes mellitus. Int J Clin Pharmacol Res 2002;22(3-4):89-99.
  16. Crespo N, Illnait J Mas R, et al. Comparative study of the efficacy and tolerability of policosanol and lovastatin in patients with hypercholesterolemia and noninsulin dependent diabetes mellitus. Int J Pharmacol Res 1999;19(4):117-27.
  17. Castano G, Mas R, Fernendez JC, et al. Comparison of efficacy and tolerability of policosanol with atorvastatin in elderly patients with type II hypercholesterolemia. Drugs Aging 2003;20(2):153-63.
  18. Plat J, Mensink RP. Plant stanol and sterol esters in the control of blood cholesterol levels: mechanism and safety aspects. Am J Cardiol. 2005; 96(1A):15D-22D.
  19. Moruisi KG, Oosthuizen W, Opperman AM. Phytosterols/stanols lower cholesterol concentrations in familial hypercholesterolemic subjects: a systematic review with meta-analysis. J Am Coll Nutr 2006 Feb;25(1):41-8.
  20. Lau VW, Journoud M, Jones PJ. Plant sterols are efficacious in lowering plasma LDL and non-HDL cholesterol in hypercholesterolemic type 2 diabetic and nondiabetic persons. Am J Clin Nutr 2005 Jun;81(6):1351-8.
  21. Heber D, Yip I, et al. Cholesterol lowering effects of a proprietary Chinese red-yeast-rice dietary supplement. Am J Clin Nutr. 1999; 69(2):231-6.
  22. Li JJ, Hu SS, et al. Effects of xuezhikang, an extract of cholestin, on lipid profile and C-reactive protein: a short-term time course study in patients with stable angina. Clin Chim Acta. 2005; 352(1-2):217-24.
  23. Heber D, Lembertas A, Lu QY, et al. An analysis of nine proprietary Chinese red yeast rice dietary supplements: implications of variability in chemical profile and contents. J Altern Complement Med 2001; 7:133-139.
  24. Harris WS. N-3 fatty acids and serum lipoproteins: human studies. Am J Clin Nutr. 1997; 65(5 Suppl):1645S-1654S.
  25. Pins JJ, First SM, et al. The effects of the dietary supplement pantethine on blood lipids and body composition in generally healthy dyslipidemic adults. FASEB Journal 19(4), A417. 2005.
  26. Moreyra AE, Wilson AC. Effect of combining psyllium fiber with simvastatin in lowering cholesterol. Arch Intern Med 2005; 165(10):1161-6.
  27. Warshafski S, Kamer RS. Effect of garlic on total serum cholesterol: A meta-analysis. Ann Intern Med 1993; 119(7 Pt 1):599-605.
 
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