Citrus Bergamot: Can give many benefits of a prescription statin medication without side effects

2022 has not been good for Joyce, a dear friend of mine. She turned 80 years old and two weeks later was informed that her breast cancer had returned and spread to her bones. Luckily, she has responded very well to the medications they are giving her to suppress it. The only issue is her "bad" cholesterol; her LDL is slightly elevated. She has been trying to get it under control for the last two years, eating a low-fat diet and walking two miles every day, but it has been refusing to drop any further.

Joyce’s family doctor recommended starting a statin medication to reduce her LDL. However, she experienced joint and muscle aches while taking estrogen-blocking medicine for breast cancer. Understandably, she is reluctant to take additional medications that could cause muscle pain or weakness and has been seeking another alternative.

Last week, her daughter suggested she try citrus bergamot. “I took citrus bergamot for 6 months, and now my cholesterol level is normal. My doctor is amazed. You should try it.”

Citrus bergamot has been getting a lot of attention recently, which it deserves. This lesser-known citrus fruit can give many benefits of a prescription statin medication without troublesome side effects like muscle pain and weakness. Pharmaceutical scientists are very excited about how bergamot extracts could reduce complications from heart disease.

Bergamot can reduce cholesterol in 3 different ways. The first way is like statin medications. Two compounds found in bergamot are almost identical in structure to the prescription statin medications given to control cholesterol. It’s believed they block the last step in making cholesterol at the same place and in the same way as statins.

Another way bergamot lowers "bad" cholesterol is by interfering with gathering and preparing sterols, the building blocks your body needs for making cholesterol.

Metformin, a leading medication for Type 2 diabetes, works by activating a beneficial pancreatic enzyme called AMPK, resulting in reduced insulin resistance. Bergamot also boosts the action of AMPK. Less insulin resistance means lower blood sugar and blood pressure, lower “bad” cholesterol (LDL) levels and triglycerides and increased “good” cholesterol (HDL). 

Finally, bergamot reduces the inflammation of blood vessels, which can progress to atherosclerosis. It does this by inhibiting the oxidation of your bad cholesterol, LDL-C, into breakdown products that trigger inflammation of your blood vessels. In fact, unlike a statin medication, bergamot has been shown to protect the blood vessels of your kidneys and liver from atherosclerotic damage.

Could citrus bergamot be harmful?

YES, IF you take medicine that interacts with grapefruit.

Although most pills dissolve in your stomach, they don't get into your bloodstream there. Vitamins, minerals, nutrients, and medications move from your small intestine into your bloodstream with the help of special cells and molecules.

One special helper is the enzyme CYP3A4. Its job is to take apart and change the shape of certain medicines, increasing or decreasing their effectiveness.

Grapefruit juice, fresh grapefruit, and citrus bergamot contain natural compounds that inactivate the CYP3A4 enzymes in your small intestine for up to 3 days at a time. Without these enzymes working to neutralize part of each dose, you can absorb more medicine, up to 50% more.

Similar to grapefruit, bergamot may also affect the absorption of some medicines.

Unfortunately for my friend Joyce, one of her breast cancer medicines interacts with grapefruit. That means that she should NOT take bergamot because it could cause an exaggerated effect of that medicine.

Joyce asked me, “What if I took the bergamot at a separate time of the day?

“The effect of grapefruit or bergamot on the enzyme CYP3A4 lasts for over 48 hours. The only way to avoid the interaction is to avoid grapefruit and bergamot while taking an affected medication.”

Here are 4 Tips for Taking Citrus Bergamot Safely:

1. Check for a grapefruit interaction.

Any medicines affected by grapefruit can also be affected by bergamot. Look for a small sticker on the side of the prescription bottle or ask your pharmacist if it is safe to have grapefruit with your medicines.

2. Avoid red yeast rice.

Red yeast rice is the source of the original statin medicine, lovastatin. Lovastatin can be affected by grapefruit. Until we know more about bergamot, avoiding red yeast rice with bergamot is best.

3. Kick back on caffeine.

Bergamot may increase the level of caffeine in your system. If you notice shakiness or stomach burning, reduce your caffeine intake.

4. Take 500mg-1000mg daily.

Start with 500mg daily and increase to 1000mg daily as tolerated.

Dr. Louise Achey, Doctor of Pharmacy, is a 43-year veteran of pharmacology and the author of Why Dogs Can’t Eat Chocolate: How Medicines Work and How YOU Can Take Them Safely. Get clear answers to your medication questions at her website and blog, TheMedicationInsider.com. ®2022 Louise Achey