Lovastatin
About lovastatin
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 high 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.
Helpful Products
Try these helpful products which may be beneficial if taken with this medicine
- CoQ10
- Supplementing with 30 to 100 mg of coenzyme Q10 per day may maintain adequate blood levels
of this heart-healthy nutrient
- Cholesterol-lowering margarine
- Using margarines containing sitostanol (Benecol), which is made from pine tree wood pulp
and naturally occurring unsaturated sterols obtained from soybean oil (Take Control), can help
lower LDL (“bad”) cholesterol
These recommendations are not comprehensive and are not intended to
replace the advice of your doctor or pharmacist. Continue reading the full article for more
information on interactions with vitamins, herbs, and foods.
Summary of
Interactions with Vitamins, Herbs, and Foods
In some cases, an herb or supplement may appear in more than one category, which may seem
contradictory. For clarification, read the full article for details about the summarized
interactions.
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
|
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. |
Coenzyme Q10
Milk thistle*
|
May Be Beneficial: Supportive
interaction—Taking these supplements may support or otherwise help your medication
work better. |
Sitostanol
|
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: Adverse interaction—Avoid these supplements when taking this
medication because taking them together may cause undesirable or dangerous results. |
Red yeast rice
|
Check: Other—Before taking any of these supplements or eating any of
these foods with your medication, read this article in full for details. |
Grapefruitor grapefruit juice
Pomegranate juice*
Vitamin A
Vitamin B3 (niacin)
Vitamin E
|
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 In a preliminary study, supplementation with 100 mg
of CoQ10 per day reduced the severity of muscle pain by 40% in people with muscle pain caused
by a statin drug.5
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.
Vitamin B3
(niacin)
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.
Sitostanol
A synthetic molecule related to
beta-sitosterol, sitostanol, is available in a special margarine and has been shown to lower cholesterol levels. In one study,
supplementing with 1.8 grams of sitostanol per day for six weeks enhanced the
cholesterol-lowering effect of various statin drugs.10
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.11 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.12 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.13 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 a statin medication.
Interactions with Foods and Other Compounds
Food
Food increases blood levels of lovastatin.14 Lovastatin should be taken with a
meal, at the same time every day.15 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 or 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.16 The same effect might be seen from eating grapefruit as from
drinking its juice. There is one case report of a woman developing severe muscle damage from
simvastatin (a drug similar to lovastatin) after she began eating one grapefruit per
day.17 To be on the safe side, people taking lovastatin should not eat grapefruit
or drink grapefruit juice.
Pomegranate juice
Pomegranate juice has been shown to inhibit the same enzyme that is inhibited by grapefruit
juice.18 19 The degree of inhibition is about the same for each of these
juices. Therefore, it would be reasonable to expect that pomegranate juice might interact with
lovastatin in the same way that grapefruit juice does.
References
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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. Caso G, Kelly P, McNurlan MA, Lawson WE. Effect of coenzyme Q10 on
myopathic symptoms in patients treated with statins. Am J Cardiol
2007;99:1409–12.
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. Goldberg AC, Ostlund RE Jr, Bateman JH, et al. Effect of plant stanol
tablets on low-density lipoprotein cholesterol lowering in patients on statin drugs. Am J
Cardiol 2006;97:376–9.
11. Muggeo M, Zenti MG, Travia D, et al. Serum retinol levels throughout
two years of cholesterol-lowering therapy. Metabolism 1995;44:398–403.
12. 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.
13. 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.
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. 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.
16. Kantola T, Kivisto KT, Neuvonen PJ. Grapefruit juice greatly
increases serum concentrations of lovastatin and lovastatin acid. Clin Pharmacol Ther
1998;63:397–402.
17. Dreier JP, Endres M. Statin-associated rhabdomyolysis triggered by
grapefruit consumption. Neurology 2004;62:670 [Letter].
18. Sorokin AV, Duncan B, Panetta R, Thompson PD. Rhabdomyolysis
associated with pomegranate juice consumption. Am J Cardiol 2006;98:705–6.
19. Summers KM. Potential drug-food interactions with pomegranate juice.
Ann Pharmacother 2006;40:1472–3.
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It is based on scientific studies (human, animal, or in vitro), clinical experience,
or traditional usage as cited in each article. The results reported may not necessarily occur
in all individuals. For many of the conditions discussed, treatment with prescription or over
the counter medication is also available. Consult your doctor, practitioner, and/or chemist
for any health problem and before using any supplements or before making any changes in
prescribed medications.