Data provided by Applied Health
side effects, nutrient depletions, herbal interactions and health notes:
• Mevacor (Lovastatin) may affect the absorption or utilization of coenzyme Q10. Supplementation may prove beneficial. Lovastatin functions by inhibiting the enzyme HMG-CoA, 3-hydroxy-3-methylglutaryl-coenzyme A reductase, that is required for the conversion of 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonic acid. Biosynthesis of both cholesterol and coenzyme Q (CoQ) requires mevalonic acid as a precursor. Consequently, lovastatin therapy could also result in a lowering of cellular CoQ levels.1
• Use of alcohol should be limited with this medication.2
• Grapefruit and grapefruit juice may drastically increase the effects of Mevacor and should not be consumed at the same time as the medication. This medication should be taken with water.Grapefruit juice increases the bioavailability of many drugs by preventing CYP3A4-mediated first-pass metabolism in the small intestine.3
• High doses of niacin can cause muscle problems with mevacor, however the drug and niacin have been used beneficially in hypercholesterolemia. Discuss the risk versus benefits of niacin supplementation with a pharmacist.4
• Both short- and long-term use of statins increase risk of reduced blood levels of CoQ10, but daily supplementation appears to show an increase in blood levels of coenzyme 10 when taken consistently.5
• Niacin and Lovastatin are both used to treat high cholesterol. There has been conflicting evidence as to whether their interaction could be beneficial or harmful6
• As a pharmacological approach to the treatment of hypercholesterolemia niaicin has often been used in dosages ranging from one to six grams per day, usually starting with 100 mg three times daily. At such levels niacin could potentially produce adverse effects in some patients with extended use and consulting with a nutritionally-informed physician would be advisable. In particular, individuals who are also taking lovastatin should consult with their prescribing physician and/or a nutritionally oriented healthcare professional to supervise and monitor the course of treatment. While research is still limited, evidence is growing that use of inositol hexoniacinate poses fewer, though potentially similar risks; it is commonly prescribed at levels of 500 mg three times daily for the initial two weeks, and then increased to 1000 mg three times per day. Again, monitoring by an appropriate healthcare provided would be prudent.7
• Alpha-tocopherol is a potent endogenous antioxidant. Much attention has been given to its role in reducing the risk of atherosclerosis based on the theory that the pathological changes result from oxidative processes. Likewise alpha-tocopherol is often used in the treatment of cardiovascular disease. Chen et al conducted initial research into the antiatherosclerotic effects of vitamin E, through preservation of endogenous antioxidant activity and inhibition of lipid peroxidation, when used with lovastatin and amlodipine. Later, in a randomized, double-masked, crossover clinical trial Palomaki et al evaluated whether lovastatin therapy (60 mg daily) affected the initiation of oxidation of low density lipoprotein (LDL) in cardiac patients on alpha-tocopherol supplementation therapy. Twenty-eight men with verified coronary heart disease and hypercholesterolemia received 450 IU alpha-tocopherol daily with lovastatin or with placebo. They concluded that alpha-tocopherol supplementation significantly increased the antioxidative capacity of LDL when measured ex vivo, but that this benefit was partially abolished by concomitant lovastatin therapy400 IU of alpha-tocopherol, twice daily, would be an appropriate dose to counter the adverse effects of lovastatin and provide some additional benefit to the cardiovascular system. Individuals who are also taking lovastatin should consult with their prescribing physician and/or a nutritionally oriented healthcare professional to supervise and monitor the course of treatment.8
• Vitamin E supplementation of may offset the loss of Coenzyme Q10. 400 IU of alpha-tocopherol, twice daily, would be an appropriate dose.9
• Research indicates that dietary fiber, from foods such as oatmeal or fruit, can reduce gastrointestinal absorption, and thereby effectiveness, of lovastatin by binding the drug. The resulting reduction in effectiveness could increase LDL cholesterol levels.10
• Richter et al have reported that fruit pectin and oat bran have a particular tendency to interact with lovastatin.11
• While the consumption of oat bran and whole fruit might in themselves contribute to lowering cholesterol, individuals taking lovastatin should separate taking the drug from the consumption of foods high in soluble fiber by at least two hours. Foods high in soluble fiber include fruit, oats and beans; oat bran, pectin and glucomannan are highly concentrated fiber sources.The simultaneous consumption of food and lovastatin results in increased blood levels of the drug.12
• Individuals using lovastatin should take the drug at the same time every day, preferably with a meal, or at least in consistent relationship to the intake of food. Many physicians and pharmacists advise taking lovastatin with food to obtain the increased levels associated with this interaction. If prescribed a single daily dose, it should be taken with the evening meal. However, as per the above concern with fiber decreasing absorption, individuals taking lovastatin should avoid eating fiber, pectin or oat bran within two hours before or after taking the drug.13
• Niacin can be very effective and safe in lowering low-density lipoprotein cholesterol and triglyceride levels and also in increasing high-density lipoprotein cholesterol levels. In combination with other lipid-lowering drugs (eg, bile acid sequestrants), it has reduced the incidence of cardiovascular events and stopped the progression of coronary artery lesions. It may be the most cost-effective lipid-lowering agent currently available. At lower doses, sustained-release forms of niacin may also improve patient compliance.14
• The herbs Artichoke plant, Fenugreek, Garlic and Plaintain may decrease blood cholesterol levels, and therefore enhance the effects of Mevacor. Consult with your pharmacist or physician before taking them.15
• Avoid red yeast rice with mevacor, it may have additive effects or increase side effects of the drug.In a much-cited review article Garnett noted that the four commonly used HMG-CoA reductase inhibitors, lovastatin, simvastatin, pravastatin, and fluvastatin, could interact with high-dose niacin, cyclosporine, erythromycin, and gemfibrozil in a way which may result in myopathy with or without rhabdomyolysis. While the basis of these reports has been limited, it has drawn attention to the issue of potential interactions. However, other researchers have found niacin to be effective in lowering cholesterol, especially as inositol hexoniacinate, which appears to provide therapeutic efficacy with minimal risk of adverse side effects. In contrast, niacinamide is not effective for lowering cholesterol. A wide range of researchers and clinicians has supported a therapeutic approach combining niacin (or inositol hexoniacinate) and statin drugs such as lovastatin as complementary tools within an integrative approach.16
References1 Ubbink JB: The role of vitamins in the pathogenesis and treatment of hyperhomocyst(e)inaemia. J Inherit Metab Dis, 1997 Jun, 20:2, 316-25.
1 Mortensen SA, Leth A, Agner E, Rohde M. Dose-related decrease of serum coenzyme Q10 during treatment with HMG-CoA reductase inhibitors. Mol Aspects Med 1997;18(suppl):S137-44.
1 De Pinieux G, Chariot P, Ammi-Said M, et al: Lipid lowering drugs and mitochondrial function - effects of HMG-CoA Reductase Inhibitors on serum upiquinone and blood lactate/pyruvate ratio, Br J Pharmacol, 1996, 42(3):333-7.
1 Bargossi Am, Grossi G, Fiorella PL, et al: Exogenous CoQ10 supplementation prevents plasma ubiquinone reduction induced by HMG-CoA reductase inhibitors, Mol Aspects Med, 1994, 15 (suppl): 187-93.
1 In 1990 Folkers et al suggested liver dysfunction, among the many known side effects of lovastatin, can be caused by the lovastatin-induced deficiency of CoQ10. Coenzyme Q10 is a component of the LDL + VLDL fractions of cholesterol which plays a key role as an essential mitochondrial redox-component and endogenous antioxidant. Much attention has been given to its role in reducing the risk of atherosclerosis based on the theory that the pathological changes result from oxidative processes. Likewise Q10 is often used in the treatment of cardiovascular disease
1 Folkers K, et al. Proc Natl Acad Sci U S A. 1990 Nov;87(22):8931-8934; Willis RA, et al. Proc Natl Acad Sci U S A. 1990 Nov;87(22):8928-8930
1 Palomaki A, et al. FEBS Lett 1997 Jun 30;410(2-3):254-258; Palomaki A, et al. J Lipid Res. 1998 Jul;39(7):1430-1437
2 Pronsky, ZM, et al: Food-Medication Interactions, Pottstown, PA, 11th edition, 1999
3 Kantola T, Kivisto KT, Neuvonen PJ. Grapefruit juice greatly increases serum concentrations of lovastatin and lovastatin acid. Clin Pharmacol Ther 1998;63:396-402.
3 Pronsky, Z Food Medication Interactions, 11th edition, 1999
3 Bailey DG, et al. Br J Clin Pharmacol. 1998 Aug;46(2):101-110
4 McKevoy GK, ed. AHFS Drug Information. Bethesda, MD: American Society of Health-System Pharmacists, 1998
4 Pronsky, Z Food Medication Interactions, 11th edtion, 1999
4 Garnett WR. Interactions with hydroxymethylglutaryl-coenzyme A reductase inhibitors. Am J Health Syst Pharm 1995;52:1639-45.
4 Malloy MJ, Kane JP, Kunitake ST, Tun P. Complimentarity of colestipol, niacin, and lovastatin in treatment of severe familial hypercholesterolemia. Ann Intern Med 1987;107:616-23.
5 Folkers K, et al. Proc Natl Acad Sci U S A. 1990 Nov;87(22):8931-8934; Willis RA, et al. Proc Natl Acad Sci U S A. 1990 Nov;87(22):8928-8930
5 Laaksonen R, et al. Eur J Clin Pharmacol 1994;46(4):313-317; Mortensen SA, et al. Mol Aspects Med. 1997;18 Suppl:S137-144;
5 ; Palomaki A, et al. FEBS Lett 1997 Jun 30;410(2-3):254-258; Palomaki A, et al. J Lipid Res. 1998 Jul;39(7):1430-1437
6 Canner PL, et al. J Am Coll Cardiol. 1986 Dec;8(6):1245-1255; Malloy MJ, et al. Ann Intern Med 1987;Nov;107(5):616-623;
6 Garnett WR. Am J Health Syst Pharm 1995 Aug 1;52(15):1639-1645; Berge KG, et al. Eur J Clin Pharmacol. 1991;40 Suppl 1:S49-51
6 Brown BG, et al. Am J Cardiol. 1997 Jul 15;80(2):111-115
7 Head KA. Alt Med Rev 1996;1:176-184
7 Murray M. Am J Natural Med 1995;2:9-12 Murray and Pizzorno, 1998, p. 354
7 Dorner Von G, et al. Arzneimittelforschung 1961;11:110-113
7 Grundy SM, et al. J Lipid Res. 1981 Jan;22(1):24-36; Carlson LA, Oro L. Atherosclerosis 1973 Jul-Aug;18(1):1-9; Canner PL, et al. J Am Coll Cardiol. 1986 Dec;8(6):1245-1255
8 Chen L, et al. J Am Coll Cardiol. 1997 Aug;30(2):569-575; Palomaki A, et al. Arterioscler Thromb Vasc Biol 1999 Jun;19(6):1541-1548.)
9 Baum H. New Scientist May 24, 1991, 24.
10 Pronsky ZM. 1995, 121
11 Richter W, et al. Lancet 1991;Sep 14;338(8768):706
12 Threlkeld DS, ed. Sep 1998; Pronsky ZM. 1995, 121.
13 Threlkeld DS, ed. Sep 1998; Pronsky ZM. 1995, 121
14 Brown BG, Zambon A, Poulin D, Rocha A, Maher VM, Davis JW, Albers JJ, Brunzell JD. Use of niacin, statins, and resins in patients with combined hyperlipidemia. Am J Cardiol 1998 Feb 26;81(4A):52B-59B
15 Newall CA, Anderson LA, Phillipson JD. Herbal Medicines A Guide for Health-care Professionals. London: The Pharmaceutical Press, 1996.
15 Facts and Comparisons,The Review of Natural Products, Clinisphere 2.0, Wolters Kluwer Company, 2000
15 PDR for Herbal Medicines, 2nd edition, Medical Economics Company, 2000
16 Heber D, Yip I, Ashley Jm, et al. Cholesterol-lowering effects of a proprietary Chinese red-yeast-rice dietary supplement. Am J Clin Nutr 1999;69:231-36.
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The information in Drug Watch is provided as a courtesy to NewsTarget readers by Applied Health Solutions in cooperation with Healthway Solutions. Although the information is presented with scientific references, we do not wish to imply that this represents a comprehensive list of considerations about any specific drug, herb or nutrient. Nor should this information be considered a substitute for the advice of your doctor, pharmacist, or other healthcare practitioner. Please read the disclaimer about the intentions and limitations of the information provided on these pages. It is important to tell your doctor and pharmacist about all other drugs and nutritional supplements that you are taking if they are recommending a new medication. Copyright © 2007 by Applied Health Solutions, Inc. All rights reserved.