The interaction of drugs with grapefruit juice: how dangerous is this for life?

The interaction of drugs with grapefruit juice: how dangerous is this for life?

If you did not know that you should not drink medicines with grapefruit juice, then read the article. This will help to warn yourself and your loved ones against unpleasant health consequences.

Recently, scientists conducted experiments, made a discovery, and decided to warn the public about a potentially dangerous interaction between many medicines and a conventional food product - grapefruit juice. It differs from medicinal interactions with each other. After all, a pharmacist in a pharmacy before issuing drugs should ask for a prescription. If it is not, then when the pills are released, the pharmacist can collect a medical history, or at least ask how a person is going to take certain drugs.

The saleswoman in the supermarket is unlikely to do the same, selling grapefruit juice. Although from this product, with simultaneous use with tablets, one can expect absolutely identical effects that cause, for example, antibiotics, relatively many other drugs. The question arises: who should warn people against danger, and is it really so harmful to the body? Look for answers to these questions below.

The interaction "Grapefruit juice is medicine": how dangerous is this?

The interaction
The interaction "grapefruit juice - medicine" is dangerous

As a rule, attention is always focused on those drug interactions that increase the concentration of medicines in the blood serum for 30-50%. For example, they always warn of the undesirable interaction of cimetidine with phenytoine or propranolol. In this case, interaction with a publicly accessible ordinary food product, which causes an increase in the concentration of medicines on 240-900%(!), does not cause serious concern of doctors.

  • A pronounced mechanism for the interaction of grapefruit juice and low bioavailability preparations, which are metabolized by the cytochrome of the intestinal wall of the P450, are very reminiscent of those processes that take place with erythromycin.
  • Both this drug and grapefruit juice increase the concentration of felodipine (dihydropyridin antagonist of hypotensive calcium) in the blood almost three times.
  • Under the influence of grapefruit juice, the peak concentration of the drug in plasma increases by an average of five times (reaching 900%), the concentration of cyclosporin (selective immunosuppressant) - three times, terphenin (antihistamine) - in 7-10 times.
  • The pharmacokinetics of midazolam (tranquilizer) also change significantly.

Important: An increase in the concentration of felodipine in the blood under the influence of juice in hypertension patients is accompanied by an increase in the hypotensive effect 2 times and an increase in heart rate. As a result, the severity of side effects increases several times.

This action is the result of significant inhibition in the intestinal wall of the cytochrome P450, which plays a key role in the metabolism of all dihydropyridine preparations, cizapride (prokinetics), midazolam, terphenin and cyclosporine. Significant inhibiting also occurs enzyme CYP1A2which affects the exchange of warfarin and caffeine. Both of these enzymes, in turn, act both on Theophylline and Imipramine.

It is worth remembering: Wallowing tablets with grapefruit juice Causes an overdose drugs! With caution, you need to eat the fruits themselves while taking medications.

The erroneous belief is that a lot of grapefruit juice needs to drink a lot of grapefruit juice to the appearance of negative effects. However, all the described effects, as a rule, caused a regular glass of this drink.

Remember: Repeated portions of juice significantly enhance the effect, and the effect of one portion can last more than a day.

Ways to attract public attention: why is it dangerous to drink medicines with grapefruit juice?

The interaction
The interaction "grapefruit juice - medicine" is dangerous

Scientists from America, who are authors of removing the danger of drug drinking with grapefruit juice, turned to their Canadian and American controls for the use of medicines and food products (FDA - organization for the quality of US food and medicine) yet in 1995. In January 1996 They distributed through the Internet the results of correspondence with these regulatory authorities and other materials regarding this problem. Such methods of attracting public attention did not work.

Then, already at the beginning of the two thousandth years, a case of death from terphenadin intoxication was known, which became a consequence of interaction with grapefruit juice:

  • A 29-year-old man from Michigan in connection with the presence of allergic rhinitis, he took more than a year, twice a day terphenin. He also had the habit of drinking 2-3 times a day, sometimes even more often, freshly squeezed grapefruit juice.
  • In September 2003, he felt bad on the street, darted to the house, but fainted and died almost instantly.
  • After death, an investigation was conducted, tests were taken. The result stunned doctors: the levels of the terphenin in serum were 35 ng/ml, in gastric juice - 78 ng/ml, and the indicators of the terphenadinic metabolite reached 130 ng/ml.
  • Such high indicators are described in other cases of fatal arrhythmia due to terphenadin.

The pathologist associated the death of this person with terphenadin intoxication. It is important that the patient did not take any other drugs that could affect the metabolism of the drug. Alcohol levels in the patient's blood did not exceed the limits of the norms for driving a car. He was also sick with cardiomegaly and hepatomegaly. However, there was no data on a violation of the liver function.

That is why it is dangerous to drink medicines with grapefruit juice. After this incident, people became more often interested in doctors whether this product really works so if it is taken with medicines. In addition, doctors of the whole world started talking about the fact that drugs should be washed down only with clean water, and not juices, compotes or other drinks.

Subsequent attempts to convince WHO and FDA about the need to warn people that drinking medicines with grapefruit juice is dangerous for life: what did this led to?

Drinking medicines with grapefruit juice is life threatening
Drinking medicines with grapefruit juice is life threatening

FDA And WHO They already knew about the aforementioned case and his connection, according to the pathologist, with terphenadin intoxication. But the connection with the simultaneous use of grapefruit juice was not installed in a timely manner. Subsequent attempts to convince WHO and FDA about the need to warn people that it is dangerous to drink medicines with grapefruit juice for life.

As a result, the consideration of this issue was sent FDA, in the cardiovascular compartment. The consideration was detailed. After that, it was concluded that significant problems can be expected with the use of drugs that have:

  • Narrow therapeutic index
  • Low bioavailability
  • Metabolism that is carried out by the enzyme CYP3A4 of the intestinal wall

Subsequently, information about this case was sent to the Allergological Department of the FDA. However, even a year after that case, officially people were still not warned.

Patients should know: what will happen if the medicine is drinking with grapefruit juice?

Drinking medicines with grapefruit juice is life threatening
Drinking medicines with grapefruit juice is life threatening

The severity of interaction can be different. Sick patients should know that sometimes such a probability is moderately increased. It can cause significant pharmacokinetic or pharmacodynamic interactions, however, without significant side effects. An example of this interaction is 30%-an increase in the concentration in the blood serum during the interaction of nifedipine and grapefruit juice. What will happen if other drugs have a grapefruit juice:

  • The interaction between this juice and felodipine is more dangerous, when the indicators of the content of the substance in the blood increase on average by 284% (maximum 600%).
  • In addition, the effect on blood pressure and heart rate doubles.
  • When interacting with nisoldipin, the peak concentration in the serum grows on 500% (maximum 900%). In such circumstances, the interaction will be accompanied by side effects of different severity - from the feeling of heat on the face and swelling of the ankles, to the general weakness and ischemia of myocardium.

In such a situation, the warning of doctors and pharmacists and the warning of patients about the likely effect of grapefruit juice is quite justified. Annotation on the drug should contain information with such a warning.

Remember: Do not drink medicines with grapefruit juice. It is forbidden to do this, both freshly squeezed and juices from the store that contains the juice of this fetus. Drink the drugs only with water!

If the interaction is difficult to control, and this can provoke significant, potentially dangerous effects, then it is advisable to warn the public. So, for example, the interaction of grapefruit juice with terphenadin can provoke arrhythmia - trembling/flickering of ventricles. It can also be expected that under the influence of grapefruit juice, significant side effects of itraconazole and lovastatin (rabdomyolysis) will be observed. Elongation sT segment With the use of cizapride, it can also progress under the influence of this juice.

How to warn people that grapefruit juice cannot be washed down with medicines: options

It is necessary to warn people that the juice of grapefruit cannot be washed down with medicines
It is necessary to warn people that the juice of grapefruit cannot be washed down with medicines

Naturally, all people should be warned that the juice of grapefruit cannot be washed out. Public attention can be attracted using the following options:

  • Messages in print and electronic media.
  • Editorial comments on different sites.
  • Advertising appeals in medical journals.
  • Instructions for medicines from manufacturers with relevant information.
  • The coordinated work of pharmacological control organs.
  • Marking of medicines and food with warnings.
  • Placing posters with a warning directly in pharmacies and stores.

Perhaps, after such actions, people will understand and remember that drinking drugs with grapefruit juice is dangerous for health and life. It is worth remembering that any tablets, syrups and other medications must be recorded only with ordinary water. Listen to such advice of doctors and scientists so as not to lose the most precious thing that every person has health. Good luck!

Video: Grapefruit. Benefits and harm.

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