Why Do Statins Fight with Grapefruit?

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.

 

Interaction Between Food and Blood Thinners

Blood thinners are the second most common medication that can interact with food and supplements. Blood thinners such as warfarin are used to prevent blood clots in people with atrial fibrillation, artificial heart valves, and deep vein thrombosis.

When a blood thinner is prescribed, people are given a list of foods and supplements to avoid. Top of the list is vitamin K and foods that contain vitamin K such as green leafy vegetables. Herbs such as garlic and ginkgo, supplements that contain vitamin E, coenzyme Q10, and omega-3 fatty acids are also discouraged because they may make the blood thinner. The goal is to optimize the international normalized ratio (INR), a measure of clotting ability. It isn’t that those types of patients have blood that coagulates more than normal; the theory is that keeping vitamin K from interfering with the blood thinner will reduce the probability of clots.

The problem: the recommendations are not supported by definitive research; it’s more a matter of playing it safe based on the theory of what the nutrients will do rather than actually based on science. In a recent review article, the authors concluded: “Restriction of dietary vitamin K intake does not seem to be a valid strategy to improve anticoagulation quality with vitamin K antagonists. It would be, perhaps, more relevant to maintain stable dietary habits, avoiding wide changes in the intake of vitamin K.” I absolutely agree.

What do you do? First, decide what diet you want to eat and supplements you want to take and stick to it. Second, work with your physician to adjust the blood thinner to get the dosage just right to keep your INR within range. Third, if you can’t get it normalized, there may be other factors as yet unknown that are affecting clotting. You’ll have to stick to the common recommendations, science-based or not.

Last chance to become an Insider and listen to tonight’s free conference call and get your health questions answered. You can learn more and join at this link.

What are you prepared to do today?

Dr. Chet

 

Reference: Medicine (Baltimore). 2016 Mar;95(10):e2895.

 

Food-Medication Interactions

One of the questions I got after Saturday’s Memo was about how to take thyroid medication to maximize effectiveness. It was of those smack-your -forehead moments—how could I forget that? This week’s Memos will cover food interactions with the three most common medications. Your physician and pharmacist should handle the medication-to-medication interactions; I’ll stick to food, including supplements. Let’s begin with synthetic or natural thyroid medications.

In order to maximize absorption of thyroid medication, take it on an empty stomach, preferably in the morning. Wait about an hour before eating.

If you take a multimineral with calcium and iron or a stand-alone calcium supplement, wait at least four hours before you take it. The range of medication loss is 25% to 35% when taken with calcium. But even more important is to be consistent in when you take your medications, when you eat, and when you take your supplements.

Next I’ll cover blood thinners.

The next Insider Conference Call is Thursday might. If you want to attend as well as listen to prior Conference Calls, sign-up as an Insider before then.

What are you prepared to do today?

Dr. Chet

 

Treating an Underactive Thyroid

The treatment for an underactive thyroid is pretty simple. Levothyroxine is a prescription medication that will work for most people. It takes time to get the dosing adjusted to get the thyroxin blood levels into a normal range. After that, it’s monitored over time and the dose is adjusted when needed.

It’s a simple process, except for those who refuse to take the medication because it’s a chemical sold as a medication. Let’s take a look at that issue.

Levothyroxine versus Thyroxin (T4)

I check the chemical structure of the synthetic and natural forms of thyroxin: they’re chemically identical with the exception of a single ion. Instead of a hydrogen ion in one bond, a sodium ion is used. That’s it. The function is the same. Not similar—the same. Levothyroxine is processed and eliminated the exact same way. While it’s made in a pharmaceutical plant, there’s no substantive difference in chemical structure or function.

There’s no reason to fear taking this medication; I do and Paula does as well. While many medications are completely synthetic and do things the body does not do, this is not one of them. However, for some people, there’s a natural alternative as long as they have no objections to pork products.

Armour Thyroid

Before the invention of levothyroxine, physicians prescribed ground thyroid glands of cows and pigs; pig thyroid is the typical source. The difference between desiccated swine thyroid and levothyroxine is that Armour thyroid contains both T4 and T3 (triiodothyronine.) The problem is that they’re not in the same ratio as found in humans, and that can make regulating thyroid hormone levels tricky.

There is one exception, other than personal preference. I got an email from a long-time reader who said she takes the Armour thyroid because levothyroxine just didn’t work. Since taking the Armour thyroid, her hormone levels are all within range.

Why would that be? My guess is that some people do not convert T4 to T3 effectively; therefore they would need both hormones, and Armour thyroid supplies both.

The Bottom Line

Based on the chemical structure and function, levothyroxine is the logical choice to treat an underactive thyroid. As I stated earlier, one ion does not make this the typical pharmaceutical; it’s as close to nature as I’ve seen. However, for those who cannot get their thyroid under control, it’s nice to have Armour thyroid as an alternative.

If you want to treat an underactive thyroid, those are the choices. There are no dietary supplements that can replace thyroid hormones. The prescription synthetic will work for just about everyone, and it makes no sense to avoid it. The truth is in the chemistry.

What are you prepared to do today?

Dr. Chet

 

Do You Have an Underactive Thyroid?

The weather in Grand Rapids has taken a turn to winter: from 61 degrees on Tuesday to freezing today. It’s bone chilling with winds at 20 mph and can leave you feeling cold most of the day. But what if you were cold most of the time regardless of the outdoor temperature? That’s just one of the symptoms of an underactive thyroid, also called hypothyroid.

Before I met with a potential coaching client to discuss his nutrition and training, I asked him when he had his last physical and how his health has been. One of the things he mentioned was feeling more fatigued than he had in the past and that it took longer to recover. Fatigue and feeling tired are also symptoms of an underactive thyroid. Those symptoms aren’t always present, and there are other explanations for those symptoms, but hypothyroid is a possibility. Here are some of the other symptoms of an underactive thyroid:

  • Trouble sleeping
  • Difficulty concentrating
  • Weight gain
  • Dry skin and hair
  • Depression, as I mentioned Tuesday
  • For women: frequent, heavy periods
  • Muscle fatigue and painful joints

There could be other explanations, but it’s a place to begin and it’s often part of a routine blood test. Schedule an appointment and have your thyroid levels checked. If your thyroid is underactive, the question I asked Tuesday applies: should you take the medication or are there alternatives? I’ll get into that on Saturday.

What are you prepared to do today?

Dr. Chet

 

What Your Thyroid Does

A common question: “I’ve just been diagnosed with an underactive thyroid. What can I do? I don’t want to take medication. I want a natural solution.” Usually, there’s a spicy descriptor that precedes the word medication. In response, the Memos this week are about the thyroid: What does it do? What happens if it doesn’t function properly? What are the treatment options?

The thyroid gland is a butterfly-shaped gland that resides on the front of the neck just above the collarbone. The best word to describe what the thyroid does: metabolism. How does it do that? By producing the hormones thyroxine (T4) and triiodothyronine (T3). It’s actually an elegant process that includes the hypothalamus and pituitary glands. The hypothalamus monitors the blood for status reports. When it senses a need for an increase in thyroid hormones, it signals the pituitary and the pituitary releases thyroid stimulating hormone (TSH), which tells the thyroid to increase the release of hormones.

Back to metabolism. That’s the rate at which cells function from calories burned, heart rate, muscle growth and repair, and many other processes. If the thyroid starts to fail, it can wreak havoc just about everywhere in your body. That’s what we’ll talk about on Thursday.

What are you prepared to do today?

Dr. Chet

 

Guidelines for Lowering Your Blood Pressure

When guidelines for any condition are changed, especially one as common as high blood pressure (HBP), it raises several questions. One question would be: is this is just a way for the medical and pharmaceutical businesses to promote and sell more drugs? Another would be: will this throw more people into the pre-existing condition category and thus hinder their ability to get health insurance? I can’t answer those questions, but I can condense the American Heart Association’s 481-page guidelines to a few points.

Environmental Causes of HBP

The nice thing, if you can call it that, is that most of the causes of HBP, also known as hypertension, are environmental; they’re caused by the way we interact with our environment in a personal way. I’ve listed the causes in the order presented in the AHA’s guidelines; they’re not ranked by significance.

  • Being overweight or obese contributes to HBP. Going back to the insurance actuarial tables, there is a distinct relationship between excess body fat and HBP. This observation has been confirmed in several large epidemiological studies over the years. If you carry extra body weight, your risk for HBP is higher.
  • Excess sodium intake is associated with HBP. The reasons can vary, but let’s look at it this way. Cells must be in a specific ionic balance to function properly. If one ion, sodium, is increased, the body must retain more fluid to keep the ionic balance. When fluid levels go up, there’s an increase in the force exerted against the inside of the arteries to handle the extra fluid. Hence, blood pressure goes up.
  • One that may surprise you is that a decreased potassium level is also associated with HBP. As a nation, we are potassium poor because we don’t consume the necessary plant material in the form of vegetables and fruit. Potassium is also an ion involved in many strategic chemical reactions. Because we take in much more sodium than potassium, the balance is thrown off and BP increases.
  • Fitness level directly affects the cardiovascular system; when fitness declines, everything from the heart’s ability to contract to the number of small blood vessels is modified in a negative way. That can increase BP.
  • Finally, excess alcohol intake is related to an increase in BP. While a little alcohol may be beneficial to help reduce stress levels, too much can increase BP.

Let’s take a look at the treatment recommendations for Elevated and Stage 1 Hypertension.

Treatment Recommendations

The initial recommendations for Elevated BP and HBP Stage 1 are lifestyle recommendations. The goal in both cases is to see how the person responds to lifestyle changes first before any medications are recommended.

There is one exception: if the person’s 10-year risk for a heart attack and stroke is greater than 10%, the recommendation is lifestyle plus medication. You can take this assessment at the link in the second reference to determine your risk. However, most physicians will give you three to six months to change your lifestyle, and then reassess whether you need the medication at all.

The important point is that it’s lifestyle change that’s recommended first, not medications. So how are you going to reduce your risk?

Lifestyle Modifications to Lower BP

  • Lose weight. There’s no single correct way to do that. Use the DASH Diet or go low fat, follow the USDA MyPlate plan or go ketogenic, use the AHA guidelines or go low carb. Whatever you can do to lose weight and keep it off, do it. For every kilo (2.2 pounds) you lose, you can expect BP to decrease by 1 mmHg, both systolic and diastolic (top and bottom numbers).
  • Eat healthier by following the DASH Diet. It focuses on vegetables, healthier fats, more fruit, nuts, fish, and whole grains. You can expect to decrease BP from 3 to 11 mmHG.
  • Reduce sodium intake to 1,500 mg per day. If that’s too difficult, shoot for a reduction of 1,000 mg per day from your current intake. Expect to reduce BP between 2 and 6 mmHg.
  • Increase potassium intake by eating more foods containing potassium—and the best source is most vegetables. It’s more than just eating bananas! Expect to reduce BP by 2 to 5 mmHg.
  • Exercise regularly and that means 4 to 5 days per week. Aerobic gets the biggest results, but weight training and even isometric exercise will reduce BP between 4 and 8 mmHg. Fun activities like dancing, tennis, and playing with the grandkids count as exercise if you keep moving and increase your heart rate.
  • Reduce excess alcohol intake. Men should have no more than two drinks per day while women should have no more than one. Expect to reduce BP 3 to 4 mmHg.

Any one of these lifestyle changes doesn’t seem too hard, but you’ll get the best results by combining a few changes. As always, I’d advise a stepwise approach: change one thing, and a week or two later change another one. If you do that and stick with it, you can reduce your BP by 10 to 15 mmHg and that will get you into the desirable range—no medication necessary.

The Bottom Line

I think the new guidelines for diagnosing and treating BP are spot on. The emphasis is on lifestyle first and foremost, so these guidelines have put the ball squarely in your hands. Take the ball and run: change your lifestyle, for good. The real benefits will be how much better you’ll feel and the knowledge that you’ve reduced your risk of heart disease and stroke considerably.

What are you prepared to do today?

Dr. Chet

 

References:
1. Hypertension. 2017;00:e000-e000.
2. http://www.cvriskcalculator.com.

 

Blood Pressure: Getting It Right

The change in the clinical guidelines for diagnosing high blood pressure, as described in Tuesday’s memo, requires that your BP reading is done correctly. That could be a problem.

In a JAMA Medical News report published in August, medical students were asked to take the BP of volunteers. Only one out of 159 got all the steps correctly. It’s not that they were poor at the actual mechanics of taking the BP, but they didn’t follow all 11 steps. Yes, 11 steps. Here they are:

  1. Five minutes of rest; that eliminates the rise in BP from getting to the office, checking in, getting weighed, etc. This is the step most often missed.
  2. The correct size cuff should be used. If your upper arms are large, and the nurse or doctor doesn’t use a large cuff, your BP reading will be higher. That’s because the bladder inside the cuff will have an artificially high pressure, which is reflected in the reading.
  3. The cuff should be placed over a bare arm, not over clothing. It’s your job to remember to wear something with a loose sleeve that won’t get in the way.
  4. The arm should be supported on a desk or a table, not hanging free.
  5. The patient should be asked not to talk. The doctor has to be able to hear the sounds clearly to get an accurate reading. This is not the time to discuss new restaurants.
  6. Legs should be uncrossed because that can affect blood flow.
  7. Feet should be flat on the floor.
  8. No reading or cell phones during measurement. There are a couple of reasons for this one. Holding the phone or book is an isometric contraction albeit a small one; nevertheless, it can raise the BP reading. The other reason is that if you’re checking email or something like that, it can affect your reading if your heart rate gets elevated.
  9. The BP in both arms should be checked.
  10. The arm with the higher reading should be noted.
  11. Finally, the physician should note in the records which arm is to be used in future readings.

Who knew taking a BP was so complicated? The photo above gets at least three steps wrong. Now that you know, you can make sure you do your part whether you’re told to or not.

But what’s going to happen if you hit higher numbers? I know many people suspect this is just a way to push more BP meds. We’ll look at treatment regulations on Saturday.

What are you prepared to do today?

Dr. Chet

 

Reference: JAMA Online. Abassi 08-30-2017.

 

Do You Have High Blood Pressure?

On Monday November 13, you may have awakened with normal blood pressure, and by that afternoon, you may have joined the ranks of those with high blood pressure (HBP). That’s when the American Heart Association (AHA) released their new HBP clinical practice guidelines at their national conference. With the new guidelines, close to half of all adults will be diagnosed with HBP.

The guidelines are the topic for this week’s Memos. I downloaded the entire document—all 481 pages—and three important parts warrant discussion. The first is AHA’s new guidelines for diagnosing HBP, and those numbers are in the graphic above.

While there are numerous questions, the first one is this: is your BP being taken correctly? That’s the topic for Thursday’s Memo, and you’ll be surprised at how often it’s done poorly.

What are you prepared to do today?

Dr. Chet

 

Reference: Hypertension. 2017;00:e000-e000.

 

Thanksgiving Wishes

I got a few questions about the safety of microwaving after my Memos on nutrients in broccoli. In doing the research, I saw no evidence that there were any changes to the chemical composition of the vegetables. The science clearly demonstrates that the phytonutrients were not altered nor decreased. I know the Internet says crazy stuff about microwaves, but the science just doesn’t support any negative effects on the food itself.

I’m not a fan of cooking elaborate meals in a microwave because the heat is not distributed equally, but for steaming veggies and reheating leftovers, no problem. If you really want to maximize your nutrients, save any of the water remaining in the pans or containers for making soup. If minerals or other nutrients leach out, that’s where they’ll be.

Happy Thanksgiving!

Paula and I would like to wish you all a very Happy Thanksgiving. Because this is a busy time of the year, this will be the only Memo this week. Enjoy family and friends—and make sure you eat your vegetables, no matter how you decide to prepare them.

And here’s a tip for easier digestion: abide by the Golden Rule of dinnertime and don’t discuss politics or religion. Especially this year.

What are you prepared to do today?

Dr. Chet