Tag Archive for: lovastatin

The Bottom Line on Red Yeast Rice

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If you remember the last Memo, I said that the active ingredient in red yeast rice (RYR) was monacolin K, which is chemically identical to a current statin medication: lovastatin. The problem with RYR in supplements is that the amounts of monacolin K varied depending on the exact type of Monascus mold used—it could be high enough to mimic the actual medication, or it could have none. You wouldn’t know because it wasn’t standardized.

As a result, the FDA declared that RYR could not be sold in the U.S. because of the lack of information on the amount of monacolin K in the supplements and because lovastatin had already been approved as a drug. Mostly the latter.

The next logical step would be to see if the FDA set a limit on the amount of monacolin K allowable in RYR products in the U.S. They have not; they consider it a drug that shouldn’t be sold in the U.S. at all. You can still find RYR as a dietary supplement, but it should not contain enough monacolin K to really do anything to lower cholesterol. On the other hand, the European equivalent of the FDA has set a limit of no more than 3 mg of monacolin K in a daily serving. You can buy it from a European company, but technically, it’s illegal in the U.S.

In this case, it makes no sense to obtain a product in the U.S. that may or may not have monacolin K in it and which could actually contain lovastatin in it as product analytics have shown. By the way, the side effects from both forms, monacolin K and lovastatin, are identical with muscle pain and the like. Doesn’t happen to most people, but it can happen. Obviously, if you’re taking a statin, don’t add RYR without your doctor’s approval.

The Bottom Line

That’s the deal with RYR in 2025. If you don’t want to take a medication, change your lifestyle to naturally lower your cholesterol. Check with your doctor to find out the limitations that he’s putting on you as it relates to exercise intensity and then get after it. Not to lose a whole bunch of weight. Not to win the next 5K. Not every day.  But to make your heart stronger and fitter. You want natural? That’s the most natural solution to high cholesterol for most people.

What are you prepared to do today?

        Dr. Chet

References:
1. Methodist Debakey Cardiovasc J. 2019 Jul-Sep;15(3):192-199.
2. NIH NCCIH 2024. Red Yeast Rice.

It’s Back: Red Yeast Rice

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I still get questions about using red yeast rice (RYR) instead of a statin to lower cholesterol. About 15 years ago, I looked up the data, wrote about it, and tucked it away. The answer was yes—but. What does that mean? Time to review it again in case you’ve been thinking about it.

Red yeast rice is actually not a yeast, it’s a mold that is produced by the fermentation of a fungus in the Monascus family that grows on, as you may have guessed, red rice. The genera Monascus purpureus is technically a mold—a fungus that produces filaments that include many cells rather than a yeast, a single-celled fungus. From a marketing perspective, you can understand why supplement manufacturers wanted to use red yeast rice rather than red mold rice.

Did RYR as a supplement work to lower cholesterol? Yes, based on several studies done in the late 1990s. There was only one problem. The RYR contained monacolin K, a by-product of fermenting the mold on the red rice. Why is that a problem? Because monacolin K is chemically identical to lovastatin, a pharmaceutical that lowers cholesterol. While no one wants to take medications any more than they have to, the RYR was a “natural” alternative. Is it still available and moreover, is it the same RYR? I’ll let you know on Saturday.

What are you prepared to do today?

        Dr. Chet

References:
1. Methodist Debakey Cardiovasc J. 2019 Jul-Sep;15(3):192-199.
2. NIH NCCIH 2024. Red Yeast Rice.

Why Do Statins Fight with Grapefruit?

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One of the most complicated medication-food interactions is grapefruit and statins, the popular cholesterol-lowering drug. The goal of this Memo is to make sense of the research to date by answering a couple of questions.

Before I begin, let me briefly explain how a statin works. One of the many enzymes required to produce cholesterol in the body is called HMG CoA reductase. In fact, it’s the rate-limiting enzyme; it controls how much cholesterol is made. Interfere with the enzyme, and you can block the production of cholesterol. That’s what most types of statins do; they block HMG CoA reductase, thus limiting the amount of cholesterol made. If your cholesterol is too high, it goes down.

How Does Grapefruit Juice Interact with Statins?

While this is some complicated biochemistry, let’s see if I can explain it simply. There’s a series of naturally occurring enzymes produced in the small intestine called CYP 450 3A4 that modifies the statin before it’s released into the bloodstream; it controls the amount and the form of the statin that gets into your body. Grapefruit juice contains phytonutrients that interfere with the CYP 450 3A4 action, letting more of the statin get into the bloodstream more quickly. Rather than fighting, it was more of a case of helping too much.

Is that good or is it bad? The research never really specifies. The logical expectation is that it would lower cholesterol too much or because it’s not in the correct form, maybe not enough. I couldn’t find an answer to that question. The original research on grapefruit juice began in the late 1980s and seemed to end about 2004. Since then, the recommendation is if you take a statin, no grapefruit juice.

What Is the Real Concern with the Interaction?

This question perplexed me for years, but I finally found an answer: with too much of the statin available due to the interference of the phytonutrients with the CYP 450 3A4, the overabundance could lead to an increased risk of rhabdomyolysis, a breakdown of muscle tissue. Muscle pain is a frequent side effect of taking statins, so the concern makes sense. The problem is that it was never really tested in any research I could find.

On top of that, the primary studies on grapefruit juice and statins used double-strength grapefruit juice in high amounts and a high dose of statins in healthy subjects. Yes, they found that the statin levels increased. But no other measures were checked such as impact on cholesterol production or markers of muscle damage. That was the state of research for the past decade.

What If You Wanted to Boost Your Statin?

In a recently published review paper, researchers theorized on the impact of grapefruit juice on cholesterol levels and the risk of cardiovascular disease. They found that if a statin such as simvastatin was taken at the same time as grapefruit juice, it increased the absorption 260% but if taken 12 hours apart, absorption was up only 90%. With atorvastatin, the increase was 80% no matter when the grapefruit juice was taken.

Calculating the effect on benefits and hazards, when simvastatin or lovastatin are taken at the same time as grapefruit juice, the estimated reduction in LDL cholesterol is 48%, and therefore, the decrease in heart disease is 70%. If the juice is taken 12 hours before these statins, the reductions are, respectively, 43% and 66%. For atorvastatin, the reduction in LDL cholesterol is 42% and in reducing the risk of CVD by 66% (1). Without the grapefruit juice, the reduction in LDL cholesterol is 37% with a decrease in risk of CVD of 61%.

This paper uses published data from many studies to perform these calculations. It doesn’t change the message in their conclusions. The benefits from the additional reduction in cholesterol may be worth the slight risk of rhabdomyolysis, but that doesn’t mean you’ll find any change in the grapefruit juice recommendation any time soon. But at least you now know the issues and why grapefruit is not the demon it’s been made out to be.

The Bottom Line

It’s important to understand that the drug, the statin, is the abnormal thing here, not the fruit. It doesn’t seem to make any sense to modify properties of a healthy diet just to be able to take a medication. But we live in the real world. Until the pharmaceutical industry can find a way to make medications that can help us and work with a healthy diet, be prudent. If you take a statin, talk with your cardiologist about finding a way to fit citrus in your diet. You may have to limit the amount or limit the times of day you eat or drink grapefruit, but as long as the net effect is getting your lipid levels in the desirable range, there has to be a way, especially since most statins should be taken at bedtime. The research is far from clear, so it’s a case by case basis.

What are you prepared to do today?

Dr. Chet

 

Reference: http://dx.doi.org/10.1016/j.amjmed.2015.07.036.