Lovastatin

Also indexed as: Mevacor®

Lovastatin is a member of the HMG-CoA reductase inhibitor family of drugs, which blocks the body’s production of cholesterol. Lovastatin is used to lower elevated cholesterol levels. Cholestin®, a dietary supplement advertised to help maintain healthy cholesterol, but not to lower high cholesterol, contains several HMG-CoA reductase inhibitor chemicals, including lovastatin.

Safetychecker Summary for Lovastatin
(for details about the summarized interactions, read the full article)

Beneficial May be Beneficial: Depletion or interference—The medication may deplete or interfere with the absorption or function of the nutrient. Taking these nutrients may help replenish them.

Coenzyme Q10
Beneficial May be Beneficial: Side effect reduction/prevention—Taking these supplements may help reduce the likelihood and/or severity of a potential side effect caused by the medication.

Milk thistle*
Avoid Avoid: Reduced drug absorption/bioavailability—Avoid these supplements when taking this medication since the supplement may decrease the absorption and/or activity of the medication in the body.

Fiber (soluble)
Avoid Avoid: Adverse interaction—Avoid these supplements when taking this medication because taking them together may cause undesirable or dangerous results.

Red yeast rice
Check Check: Other—Before taking any of these supplements or eating any of these foods with your medication, read this article in full for details.

Niacin

Vitamin A

Vitamin E

Grapefruit juice
Supportive interaction

None known

An asterisk (*) next to an item in the summary indicates that the interaction is supported only by weak, fragmentary, and/or contradictory scientific evidence.

Interactions with Dietary Supplements

Coenzyme Q10
It has been clearly documented that HMG Co-A reductase inhibitors, including lovastatin,1 deplete coenzyme Q10 (CoQ10) levels in the blood, an effect that may be responsible for other side effects of the drug, such as abnormal liver function. In a double-blind trial, blood levels of CoQ10 were measured in 45 people with high cholesterol treated with lovastatin (20–80 mg per day) or pravastatin (10–40 mg per day) for 18 weeks.2 A significant decline in blood levels of CoQ10 occurred with both drugs. Supplementation with 90–100 mg per day CoQ10 has been shown to prevent reductions in blood levels of CoQ10 due to simvastatin.3 4 However, some investigators have questioned whether it is worthwhile or necessary for individuals taking HMG-CoA reductase inhibitors to supplement with CoQ10.5 Until more is known, people taking lovastatin should ask a doctor about supplementation with 30–100 mg CoQ10 per day.

Fiber (soluble)
Soluble fiber is found primarily in fruit, beans, and oats, but it is also available separately as pectin, oat bran, and glucomannan. Two sources of soluble fiber—pectin (found in fruit) and oat bran (a component of oatmeal also available by itself)—have been reported to interact with lovastatin.6 The fiber from these two sources appears to bind the drug in the gastrointestinal tract and reduce absorption of the drug as a consequence. People taking this drug should avoid concentrated intake of soluble fiber, as taking lovastatin with a high soluble-fiber diet leads to reduced drug effectiveness.

Niacin (Vitamin B3, nicotinic acid)
Niacin is a vitamin used to lower cholesterol. Large amounts of niacin taken with lovastatin have been reported to cause potentially serious muscle disorders (myopathy or rhabdomyolysis).7 However, niacin also enhances the cholesterol-lowering effect of lovastatin.8 Taking as little as 500 mg three times per day of niacin with lovastatin has been shown to have these complementary, supportive actions with almost none of the side effects seen when higher amounts of niacin are taken.9 Nevertheless, individuals taking lovastatin should consult with their doctor before taking niacin.

Vitamin A
A study of 37 people with high cholesterol treated with diet and HMG-CoA reductase inhibitors found serum vitamin A levels increased over two years of therapy.10 It remains unclear whether this moderate increase should suggest that people taking lovastatin have a particular need to restrict vitamin A supplementation.

Vitamin E
Oxidative damage to LDL (“bad”) cholesterol is widely believed to contribute to heart disease. In a double-blind trial, lovastatin was found to increase oxidative damage to LDL cholesterol and vitamin E was reported to protect against such damage, though not to completely overcome the negative effect of lovastatin.11 This study suggests that people taking lovastatin might benefit from supplemental vitamin E.

Interactions with Herbs

Milk thistle  (Silybum marianum)
One of the possible side effects of lovastatin is liver toxicity. Although there are no clinical studies to substantiate its use with lovastatin, a milk thistle extract standardized to 70–80% silymarin may reduce the potential liver toxicity of lovastatin. The suggested use is 200 mg of the extract three times daily.

Red yeast rice  (Monascus purpureas)
A supplement containing red yeast rice (Cholestin®) has been shown to effectively lower cholesterol and triglycerides in people with moderately elevated levels of these blood lipids.12 This extract contains small amounts of naturally occurring HMG-CoA reductase inhibitors such as lovastatin and should not be used if you are currently taking lovastatin or pravastatin.

Interactions with Foods and Other Compounds

Food
Food increases blood levels of lovastatin.13 Lovastatin should be taken with a meal, at the same time every day.14 Due to the possibility of reduced lovastatin absorption in the presence of soluble fiber, it makes sense to avoid eating fruit or oatmeal within two hours before or after taking lovastatin.

Grapefruit juice
In a small, single-dose trial with healthy volunteers, blood levels of lovastatin increased to a significantly greater extent when the drug was taken with grapefruit juice than when it was taken with water.15 The same effect might be seen from eating grapefruit as from drinking its juice. It is not known whether or not grapefruit juice can be safely used to reduce the dosage requirement for lovastatin.

References:

1. Folkers K, Langsjoen P, Willis R, et al. Lovastatin decreases coenzyme Q levels in humans. Proc Natl Acad Sci 1990;87:8931–4.

2. 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.

3. Bargossi AM, Grossi G, Fiorella PL, et al. Exogenous CoQ10 supplementation prevents plasma ubiquinone reduction induced by HMG-CoA reductase inhibitors. Molec Aspects Med 1994;15(suppl):s187–93.

4. Miyake Y, Shouzu A, Nishikawa M, et al. Effect of treatment with 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors on serum coenzyme Q10 in diabetic patients. Arzneimittelforschung 1999;49:324–9.

5. Paloma’ki A, Malminiemi K, Solakivi T, Malminiemi O. Ubiquinone supplementation during lovastatin treatment: Effect of LDL oxidation ex vivo. J Lipid Res 1998;39:1430–7.

6. Richter W, Jacob B, Schwandt P. Interaction between fibre and lovastatin. Lancet 1991;338:706 [letter].

7. Garnett WR. Interactions with hydroxymethylglutaryl-coenzyme A reductase inhibitors. Am J Health Syst Pharm 1995;52:1639–45.

8. Malloy MJ, Kane JP, Kunitake ST, Tun P. Complementarity of colestipol, niacin, and lovastatin in treatment of severe familial hypercholesterolemia. Ann Intern Med 1987;107:616–23.

9. Gardner SF, Schneider EF, Granberry MG, Carter IR. Combination therapy with low-dose lovastatin and niacin is as effective as higher-dose lovastatin. Pharmacotherapy 1996;16:419–23.

10. Muggeo M, Zenti MG, Travia D, et al. Serum retinol levels throughout two years of cholesterol-lowering therapy. Metabolism 1995;44:398–403.

11. Palomäki A, Malminiemi K, Malminiemi O, Solakivi T. Effects of lovastatin therapy on susceptibility of LDL to oxidation durgy alpha-tocopherol supplementation. Arterioscler Thromb Vasc Biol 1999;19:1541–8.

12. 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;69:231–6.

13. Threlkeld DS, ed. Diuretics and Cardiovasculars, Antihyperlipidemic Agents, HMG-CoA Reductase Inhibitors. In Facts and Comparisons Drug Information. St. Louis, MO: Facts and Comparisons, Sep 1998, 171v.

14. Threlkeld DS, ed. Diuretics and Cardiovasculars, Antihyperlipidemic Agents, HMG-CoA Reductase Inhibitors. In Facts and Comparisons Drug Information. St. Louis, MO: Facts and Comparisons, Sep 1998, 171v.

15. Kantola T, Kivisto KT, Neuvonen PJ. Grapefruit juice greatly increases serum concentrations of lovastatin and lovastatin acid. Clin Pharmacol Ther 1998;63:397–402.