Multi-Drug Resistance
Grapefruit juice could be beneficial for use with some drugs with low bioavailability.
While the consumption of grapefruit juice with a drug may cause toxic levels of that drug in the body, there are some drugs that already have such low bioavailability that grapefruit juice may help increase the metabolic dose a patient receives. Inexpensive CYP3A4 inhibitors have the potential to either seriously reduce or to enhance drug availability. Therefore, development of non-toxic and stable CYP3A4 inhibitors from components in grapefruit juice may lead to better drug treatment regimes in the future.
Specifically, substances identified within grapefruit juice that increase the bioavailability of a drug in the body could be purified and extracted. These chemicals could then be incorporated in the pill for drugs like Saquinavir to facilitate increasing the efficacy of a given drug dose while decreasing the quantity and price of that drug.
The
danger with this approach is that every individual has a unique and different
amounts of CYP3A4 and P-glycoprotein enterocyte activities. Grapefruit juice
may have a large effect on one person while having relatively little effect
on another. Furthermore, in the case of Multi-Drug Resistance problems for chemotherapy
drugs, grapefruit juice effects may vary from patient to patient. However, the
results described here and ongoing investigations are a good beginning from
which to develop better solutions than are currently available.
Educating the Public
While the public is generally aware that certain food and drug interactions exist, there is certainly a need for dissemination of more accurate and scientifically correct information. Most of the public remains ignorant to the potential gravity of grapefruit juice and drug interactions.
Information
regarding the dosage, timing, and long term consequences of consuming grapefruit
juice along with drugs should be available on the bottles of juice sold on store
shelves as well as on drug container labels. The medical community must do a
better job of informing patients about medications most likely to have deleterious
grapefruit drug interactions. A well-publicized and understandable biochemical
explanation regarding CYP3A4 and the P-glycoprotein would convey to the public
the severity of the consequences of the interactions of drug metabolism and
grapefruit juice.
A Note About Herbal Supplements
Figure 30: The myriad of vitamins and other herbal supplements availiable to consumers in the market
Health problems due to drug interactions with grapefruit juice are only one example of those that can occur with other supplements. All of these supplements exist amidst a sea of other similar herbal supplements that flood the consumer market. A recent New Yorker article entitled "Miracle in a Bottle" really strikes at the heart of the dietary supplement problem.
"This really is a belief system, almost a religion. Americans believe they have the right to address their health problems in the way that seems most useful to them. Often, that means supplements they are ready to believe anything if it brings them a little hope" (Specter, 2004).
These products, these miracles that are offered in a bottle, are cloaked in what seems like scientific validity. However, not all of these herbal combinations are benign. The significant and wholly unexpected results that are seen with grapefruit juice consumption is just one of numerous examples of herbal drug interactions that are directly pertinent to the average consumer. As seen from the research cited in this website, grapefruit juice seriously disrupts the enzymes found in the small intestine, causing high blood levels of drugs, intensifying side effects, and preventing the efficacy of the drug on the disease being treated.
The dream of wellness and the reality of wellness are oftentimes very different in the world of herbal supplements. There is no doubt that better regulation is necessary to ensure that the thousands of botanical substances currently on the market do not unwittingly harm the thousands of corresponding consumers purchasing them. Later this year, Congress will considers legislation to regulate the dietary supplement agency. Perhaps better labeling and consumer knowledge can prevent the horrible consequences that may ensue should some one take Bitter Orange along with cholesterol lowering agents. If you should find yourself wandering down a grocery aisle filled with little bottles of hope, perhaps a word to the wise would be to remember the mighty grapefruit and the danger hidden beneath the innocent exterior and leave the bottles on the shelf.
Xuemei Cai · caix@email.arizona.edu
Biochemistry 462b Honors Project · The University of Arizona
Instructor Dr. Don Bourque
Last Revised May 2004