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Using Nutraceuticals to Manage Adverse Effects of Statins

By Prof. Gene Bruno, MS, MHS, RH(AHG)
Huntington College of Health Sciences

In allopathic medicine, statin drugs (HMG-CoA reductase inhibitors) are the standard of care for treating hypercholesterolemia. Certainly, there is a significant body of research demonstrating that statins are efficacious for this purpose, although such therapy is not without its risks of adverse effects. To some extent, risk of adverse effects can be managed with the use of specific nutraceuticals.

Statins, Myopathy and Coenzyme Q10
Musculoskeletal symptoms (e.g. myopathy) are perhaps the most commonly reported adverse effects associated with statin therapy.1 Myopathy may be related in part to statin inhibition of the endogenous synthesis of coenzyme Q10 (CoQ10), an essential cofactor for mitochondrial energy production.2 Therefore, it is no surprise that studies exist showing that supplementation with CoQ10 may decrease muscular adverse effects caused by statins. In some research, patients with statin-induced myopathy who took 100 mg/CoQ10 had significantly reduced pain intensity compared to baseline and compared to a control after 30 days of treatment.2-3 Likewise, in patients taking high-dose lovastatin investigationally as a treatment for cancer, supplementation with CoQ10 decreased the dose-limiting statin toxicity of myopathy.4-It should be noted, however, that other research did not find that CoQ10 significantly improved pain associated with statin-induced myopathy compared to placebo.6-7

Statins and Beta-sitosterol Absorption
Beta-sitosterol and other plant sterols have been shown to be effective for reducing the absorption of dietary cholesterol, and subsequently reducing serum cholesterol levels.8-9 In fact, the research is so compelling that the FDA (U.S. Food and Drug Administration) has actually approved a health claim for plant sterols indicating that their consumption (in combination with an appropriate diet) may reduce the risk of heart disease by means of lowering cholesterol. In addition, there are multiple studies demonstrating the efficacy of beta-sitosterol for reduction of lower urinary tract symptoms (LUTS) in men (especially in cases of BPH).10-16

Since a 2016 systematic review and meta-analysis found that men with LUTS have an increased risk of major adverse cardiac events (P=0.01),17 it is likely that men who are using beta-sitosterol supplements for LUTS may also be using medications to help in the reduction of serum cholesterol levels. This may be problematic since the statin drug pravastatin (another cholesterol-lowering medication) can also lower blood levels of beta-sitosterol by about 60 percent after four weeks.18 Theoretically, this might occur with other HMG-CoA reductase inhibitors, although this does not seem to be the case with simvastatin.19 Likewise, the cholesterol-lowering medication ezetimibe has been shown to reduce blood levels of beta-sitosterol by about 40 percent.20-21  This being the case, in men using beta-sitosterol for LUTS, it is worth increasing the dose by 40 to 60 percent if they are also using statins or ezetimibe.

1 Backes JM, Ruisinger JF, Gibson CA, Moriarty PM. Statin-associated muscle symptoms-Managing the highly intolerant. J Clin Lipidol. 2017 Jan – Feb;11(1):24-33.
2 Caso G, Kelly P, McNurlan MA, Lawson WE. Effect of coenzyme q10 on myopathic symptoms in patients treated with statins. Am J Cardiol. 2007 May 15;99(10):1409-12.
3 Kelly P, Vasu S Getato M McNurlan M Lawson WE. Coenzyme Q10 improves myopathic pain in statin treated patients (abstr). J Am Coll Cardiol 2005;45:3A.
4 Thibault A, Samid D, Tompkins AC, et al. Phase I study of lovastatin, an inhibitor of the mevalonate pathway, in patients with cancer. Clin Cancer Res 1996;2:483-91.
5 Kim WS, Kim MM, Choi HJ, et al. Phase II study of high-dose lovastatin in patients with advanced gastric adenocarcinoma. Invest New Drugs 2001;19:81-3.
6 Marcoff L, Thompson, PD. The role of coenzyme Q10 in statin-associated myopathy: a systematic review. J Am Coll Cardiol 2007;49:2231-7.
7 Young JM, Florkowski CM Molyneux SL McEwan RG Frampton CM George PM. Coenzyme Q10 does not improve simvastatin tolerability in dyslipidemic patients with prior statin-induced myalgia. Circulation 2007;114:II41.
8 Racette SB, Lin X, Lefevre M, Spearie CA, Most MM, Ma L, Ostlund RE Jr. Dose effects of dietary phytosterols on cholesterol metabolism: a controlled feeding study. Am J Clin Nutr. 2010 Jan;91(1):32-8.
9 Hendriks HF, Weststrate JA, van Vliet T, Meijer GW. Spreads enriched with three different levels of vegetable oil sterols and the degree of cholesterol lowering in normocholesterolaemic and mildly hypercholesterolaemic subjects. Eur J Clin Nutr. 1999 Apr;53(4):319-27.
10 Klippel KF, Hiltl DM, Schipp B. A multicentric, placebo-controlled, double-blind clinical trial of beta-sitosterol (phytosterol) for the treatment of benign prostatic hyperplasia. German BPH-Phyto Study group. Br J Urol 1997;80(3):427-32.
11 Berges RR, Windeler J, Trampisch HJ, Senge T. Randomised, placebo-controlled, double-blind clinical trial of beta-sitosterol in patients with benign prostatic hyperplasia. Beta-sitosterol Study Group. Lancet 1995;345(8964):1529-32.
12 Fischer A, Jurincic-Winlder CD, Klippel KF. Conservative treatment of benign prostatic hyperplasia with high-dosage b-sitosterol (65 mg): results of a placebo-controlled double-blind study. Uroscop 1993;1:12-20.
13 Kobayashi Y, Sugaya Y, Tokue A. [Clinical effects of beta-sitosterol (phytosterol) on benign prostatic hyperplasia: preliminary study] [Article in Japanese] Hinyokika Kiyo 1998;44(12):865-8.
14 Berges RR, Kassen A, Senge T. Treatment of symptomatic benign prostatic hyperplasia with beta-sitosterol: an 18-month follow-up. BJU Int 2000;85(7):842-6.
15 Wilt TJ, MacDonald R, Ishani A.Beta-sitosterol for the treatment of benign prostatic hyperplasia: a systematic review. BJU Int 1999;83(9):976-83.
16 Wilt T, Ishani A, MacDonald R, Stark G, Mulrow CD, Lau J. Beta-sitosterols for benign prostatic hyperplasia. Cochrane Database of Systematic Reviews 1999;(3) Art. No.: CD001043; DOI: 10.1002/14651858. CD001043.
17 Gacci M, Corona G, Sebastianelli A, Serni S, De Nunzio C, Maggi M, Vignozzi L, Novara G, McVary KT, Kaplan SA, Gravas S, Chapple C. Male Lower Urinary Tract Symptoms and Cardiovascular Events: A Systematic Review and Meta-analysis. Eur Urol. 2016 Jul 20. pii: S0302-2838(16)30405-5.
18 Hidaka H, Kojima H, Kawabata T, et al. Effects of an HMG-CoA reductase inhibitor, pravastatin, and bile sequestering resin, cholestyramine, on plasma plant sterol levels in hypercholesterolemic subjects. J Atheroscler Thromb 1995;2:60-5.
19 Ntanios FY, Jones PJ, Frohlich JJ. Effect of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor on sterol absorption in hypercholesterolemic subjects. Metabolism 1999;48:68-73.
20 Salen G, von Bergmann K, Lutjohann D, et al. Ezetimibe effectively reduces plasma plant sterols in patients with sitosterolemia. Circulation 2004;109:966-71.
21 Sudhop T, Lutjohann D, Kodal A, et al. Inhibition of intestinal cholesterol absorption by ezetimibe in humans. Circulation 2002;106:1943-8.

Professor Gene Bruno, MS, MHS, the Provost for Huntington College of Health Sciences, is a nutritionist, herbalist, writer and educator. For more than 37 years he has educated and trained natural product retailers and health care professionals, has researched and formulated natural products for dozens of dietary supplement companies, and has written articles on nutrition, herbal medicine, nutraceuticals and integrative health issues for trade, consumer magazines and peer-reviewed publications. He can be reached at gbruno@hchs.edu.