I Have Been Busy Answering Emails

I have lost track of the number of emails lately, but I do appreciate them as it tells me that people are reading some of my blog postings. Plus, I enjoy being able to help people. The emails covered a variety of topics and were mainly from the last two months. There were a few topics from 2012 and 2013.

My biggest concern is the response to this and this blog. Many have concerns about why they or a parent were not told about grapefruit causing toxic medication problems for statins and heart medications. One email author said he had been told not to consume grapefruit or grapefruit juice, but his mother had not found out about it until his wife needed to take her to the hospital in serious condition one Saturday morning.

The next morning she asked for a glass of grapefruit juice and the nurse looked at the medications list and asked her if she wanted to stay in the hospital or possibly be sicker to the point of death. His mother said that grapefruit was a natural fruit and she wanted it. At that point her doctor and her son arrived and she complained about not being able to have grapefruit juice with her breakfast. Her doctor told her about the interaction with her statin, simvastatin, and that was why she was fortunate her daughter in-law had rushed her to the emergency room.

He explained the dangers and when she still insisted on the grapefruit juice, he said he would stop her statin and prescribe something else. He said she could not have grapefruit for two days because the statin needs to be out of her body before she had grapefruit or grapefruit juice. He then said he would bring something for her to read so that she could understand why she should not mix grapefruit with a statin.

When she insisted on the grapefruit juice, her doctor explained that if she had the grapefruit juice and still had the statin medication in her system, it could cause her death. She laughed and the doctor said this is why she should read the article he would bring her. He called the nurse station and had them find the article and bring it to her. When she still insisted, her son said even he had been told this by his doctor, and that was the reason he had stopped eating grapefruit.

Her son stated that even after she had read the article, she still insisted on having the grapefruit juice and when she could not, called for the nurse to dial the hospital administrator and she would give him instructions to bring her some grapefruit juice. When he would not, she told her son to get her out of the hospital even against doctor's orders.

The son stated that even when he refused, she tried to get her clothes and leave. It took her son and three nurses to restrain her. Two doctors arrived then and as she collapsed, they rushed her to the ICU unit and needed to operate shortly thereafter because she had a heart attack.

Now he is talking to the heart doctor about his mother's obsession with grapefruit juice. The doctor said that he would prescribe a medication that would not interact with the grapefruit juice.

He thanked me for writing the several blogs on this problem and polypharmacy and he may have missed this otherwise, when he was prescribed a statin and in that discussion, the doctor did make this known and was happy that he would follow the instructions. He said his mother's doctor was happy that she would not be able to drink grapefruit juice for several days and the statin should be out of her body by then.

This has become longer than I thought, but the author said he appreciated my alerting him and we have exchange several emails over the last week and he says his mother should be out of the hospital sometime Monday. He says his mother still insists on grapefruit juice, but now he does not need to worry and he or his wife will accompany her to any doctor appointments in the future. The doctor has also provided him with the current list of medications that can be adversely affected by grapefruit. He said it is almost four full pages in length.

He gave me permission to use the information.

Grapefruit Can Interfere with Prescription Medications

First, here is some positive information about grapefruit. It’s delicious when broiled with a bit of brown sugar. It’s packed with vitamin C, dietary fiber, and potassium. It’s good for the immune system, skeletal system, and the cardiovascular system!

Yes, grapefruit has some good points and is generally healthy for you. However, grapefruit has a bad side and many people fall victim to the worse side of grapefruit. Grapefruit has earned the ire of some for its potential to cause harmful drug interactions and is known as the grapefruit effect. But, why is it specifically grapefruit and grapefruit juice that’s singled out?

Even though the harmful drug interactions have been known for several decades, many doctors still do not warn patients when they prescribe a drug known to be on the list. To begin with, the chemical in grapefruit that we’re going to talk about is called furanocoumarin. It’s a toxic chemical found in many plants that functions as a line of defense against would be eaters through a bitter flavor and by causing potential stomach issues.

It’s that exact line of defense that causes the drug interaction. Furanocoumarin is also found in most other citrus; but sour oranges, some mandarins, and tangelos have higher concentrations, though not as high as grapefruit.

The chemical doesn’t interact directly with medications, but instead binds itself to an enzyme found in the liver and intestinal tract. The enzyme in question is known as CYP3A4. This enzyme helps regulate how much of a drug may enter your bloodstream.

Essentially, furanocoumarin puts CYP3A4 into a headlock; as a result, it can’t do its job, so a medication seeps into your bloodstream at an increased rate. Certain drugs show different effects. Men taking Viagra may see the drug hit harder and faster, which may sound good but likely, this may come along with headaches, dizziness or even vomiting. None of which will help sexify the mood.

The FDA notes that cholesterol lowering drugs known as statins often have harmful interactions with grapefruit juice. These can include dizziness, harm to the liver and kidneys, and muscle breakdown. In one Mayo Clinic study, some people even showed signs of memory loss.

Some psychiatric and anxiety medications have also displayed signs of the grapefruit effect, including upset stomach, digestive issues, and exhaustion.

If you’re unsure of what drugs interact with grapefruit juice you can see a partial list here. I have more in this blog and this blog.

Grapefruit, A Superfood or A Drug Nightmare?

This author creates hype for grapefruit by calling it a superfood. Then what she presents as being the new antioxidant found in the citrus – Naringenin. Naringenin is far from a proven antioxidant and the tests to date have all been performed on rats and mice. This is why I label what she says as hype.

The following is quoted from Wikipedia which is not known for being totally accurate.

"This substance, naringenin, has also been shown to reduce oxidative damage to DNA in vitro. Scientists exposed cells to 80 micromoles of naringenin per liter, for 24 hours, and found that the amount of hydroxyl damage to the DNA was reduced by 24% in that very short period of time.[citation needed]

Naringenin found in grapefruit juice has been shown to have an inhibitory effect on the human cytochrome P450 isoform CYP1A2, which can change pharmacokinetics in a human (or orthologous) host of several popular drugs in an adverse manner, even resulting in carcinogens of otherwise harmless substances.

Naringenin has also been shown to reduce hepatitis C virus production by infected hepatocytes (liver cells) in cell culture. This seems to be secondary to Naringenin's ability to inhibit the secretion of very-low-density lipoprotein by the cells. The antiviral effects of naringenin are currently under clinical investigation.

Naringenin seems to protect LDLR-deficient mice from the obesity effects of a high-fat diet.

Naringenin lowers the plasma and hepatic cholesterol concentrations by suppressing HMG-CoA reductase and ACAT in rats fed a high-cholesterol diet.

The National Research Institute of Chinese Medicine in Taiwan conducted experiments on the effects of the grapefruit flavanones naringin and neringenin on CYP450 enzyme expression. Naringenin proved to be a potent inhibitor of the benzo(a)pyrene metabolizing enzyme benzo(a)pyrene hydroxylase (AHH) in vitro experiments in mice. This suggests, but does not conclusively prove, that naringenin would elicit the same response when administered to humans. More research will be needed to determine if naringenin has any clinically significant effects (including medical applications) in human subjects." Unquote

Beverleigh H Piepers is the author of this article declaring grapefruit as being at “diabetic superfood.” What is not mentioned is that many of the people with diabetes cannot eat this superfood, especially if they are taking statins, some antibiotics, cancer drugs, and heart drugs. Most at risk are older people who use more prescriptions and buy more grapefruit.

The gist of the situation is the grapefruit, which contains furanocoumarins, blocks an enzyme that normally breaks down certain medications in the body. When this happens, medication levels in the body can become toxic.

I don't care how many concoctions for grapefruit she lists, grapefruit is not the diabetic superfood for many with diabetes. For me, grapefruit almost became a drug nightmare when my wife suggested I eat it. I did and became very sick. She then went to her drug book and discovered that grapefruit was contraindicated for the statin I was taking. At that point, I was handed a 12-ounce glass of water and told to drink it, followed by several more glasses of water. After five glasses, I could tell that I was flushing the toxin out and was starting to feel better.

This should tell you that if you are on the medications mentioned above, have a talk with your doctor about how grapefruit might affect you and interact with the medication.  Don't let grapefruit cause a nightmare for you.

Like Grapefruit? Watch for Drug Interactions

Ever had a jaw dropping moment? I did and now I know why I am not eating grapefruit or drinking grapefruit juice any longer. I did not realize this and was having some problems with a statin. My wife found something in her drug guide saying not to drink grapefruit juice if taking this drug. Now it is in WebMD (Medscape reprint), and I thank them for that. This topic was also a MedicalNews Today article in May 2006, and even then doctors were saying it was not news. I wish this would get more publicity, but the media does not think it is important enough or will generate enough interest. For anyone taking statins, this is important!

The article clearly states the problem with grapefruit, which contains furanocoumarins, (furanocoumarins are a class of organic chemical compounds produced by a variety of plants) is creating potentially fatal side effects in many drugs. The number of drugs being affected has in the last four years has risen from 17 drugs, and now stands at more than 85 drugs that may be affected by grapefruit. Seville oranges (often used in marmalade), limes, and pomelos also contain the active ingredients (furanocoumarins), but have not been as widely studied.

“The list includes some statins that lower cholesterol (such as atorvastatin, lovastatin, and simvastatin), some antibiotics, cancer drugs, and heart drugs. Most at risk are older people who use more prescriptions and buy more grapefruit.” The gist of the situation is the grapefruit, which contains furanocoumarins, blocks an enzyme that normally breaks down certain medications in the body. When this happens, medication levels in the body can become toxic. This is not presently on the FDA's list of things to watch for, but should be.

Grapefruit interacts with drugs taken orally and one 7-ounce glass of grapefruit juice used once a day for three days can affect simvastatin and makes it a 330% concentration greater than taking simvastatin with water. It does not matter if the grapefruit is taken with simvastatin or hours before you take it. This may cause muscle damage called rhabdomyolysis, which can be life threatening. Rhabdomyolysis is an acute, fulminant, potentially fatal disease that destroys skeletal muscle and is often accompanied by the excretion of myoglobin in the urine.

In addition to statins, grapefruit may interact with some antibiotics, cancer drugs, heart drugs and hormonal drugs. Many can interact and have more of a potential deadly effect if taken in close proximity to drinking grapefruit juice. Therefore, if you are taking any of the above types of drugs, remember to talk with your physician or your pharmacist to know if you need to avoid eating grapefruit or drinking grapefruit juice. Remember that the other fruits mentioned above may also need to be avoided.

This is a reminder that not all of an entire drug class may interact with grapefruit products, so be sure for your health, that you talk to your physician to possibly substitute a related drug that will not interact with your favorite fruit. Never stop taking a prescription drug unless you have talked to your doctor first. He/she may feel it is better for you not to use grapefruit than switch you to a grapefruit-friendly drug.

Grapefruit is a great aid to most diets, but always double check with you doctor or pharmacist to avoid problems of grapefruit having a dangerous interaction with the drug you are taking. A good rule is “better safe than sorry.”