Eat grapefruit contraceptive failure drug + grapefruit juice = take poison?

Now is the time when grapefruit goes on the market. The grapefruit with lots of juicy juice is loved by many people. But recently, an online madness has circulated an article, "Is it a failure to eat grapefruit contraceptives? These medicines must not be eaten with the grapefruit....” It is mentioned that if you take a variety of medicines together with grapefruit, you may experience side effects.

Zhou Quan, deputy director of the Department of Pharmacy at the Zhejiang Medical University Second Hospital, has a research on the interaction between food and drugs. He participated in the compilation of Clinical Pharmacokinetics and is an expert in the field of drug metabolism research. He said that the Internet's statement that eating yuzu after serving is equal to taking poison is inaccurate. In fact, not all grapefruit, only grapefruit will cause adverse reactions when used in conjunction with some drugs.

Experiments with grapefruit juice, honey pomelo juice and pomelo juice found that only grapefruit juice caused adverse drug reactions

Zhou Quan, deputy director, said that there are many kinds of grapefruit, not all varieties of grapefruit and drugs with food, will cause toxic side effects.

Domestic experts have done experiments to compare the pharmacokinetics of felodipine (an antihypertensive drug) with 250 ml of grapefruit juice, Guanxi honey grapefruit juice and Changshanhu grapefruit juice. The results showed that there was a clear interaction between grapefruit juice and this type of drug, which caused an increase in plasma concentration, but there was no significant effect of Guanxi honey pomelo juice and Changshan pomelo juice.

There is also a study on the interaction between pomelo and cyclosporine (an anti-organ transplant rejection drug) in foreign countries. It was found that eating 250 grams of pomelo pulp causes a slight increase in the blood drug concentration after taking cyclosporine, but the degree of interaction does not Grapefruit juice significantly increased the concentration of cyclosporine plasma as strong.

The study found that only some drugs cause adverse reactions when they are eaten with grapefruit, and other types of grapefruit such as pomelo, pomelo, etc., generally do not have significant effects. In addition, the degree of adverse drug reactions is closely related to the amount of grapefruit consumed, and when the amount of food consumed is large, adverse reactions are also large.

Eat grapefruit contraceptives will fail?

Wrong! Both efficacy and toxic side effects will increase

According to articles circulating on the Internet, studies in the United States have found that the impact of grapefruit on contraceptives is most prominent. Experts said that if a woman taking a birth control pill eats 1-2 grapefruit after sex, or if she directly delivers a pill with a large glass of grapefruit juice, she may become a mother because of the obstruction of grapefruit. Women’s absorption of contraceptives.

Zhou Quan said that this statement is wrong. In fact, the opposite is true.

"The contraceptives are mainly hormonal drugs. The drugs need to be catabolized by the metabolic enzyme CYP3A4. If they are eaten together with grapefruit or grapefruit juice, the furocoumarin in grapefruit inhibits the body's CYP3A4 production and the human plasma concentration. Will increase, in theory, the efficacy and toxic side effects will also increase."

Grapefruit and antihypertensive drugs eat him from high blood pressure to low blood pressure

A 48-year-old engineer had been admitted to the Department of Cardiology at Tongde Hospital in Zhejiang Province. This patient had suffered from high blood pressure for 5 years. One day, she suddenly experienced dizziness. Her blood pressure was only 90 mmHg/60 mmHg. The blood pressure is obviously low. The doctor carefully asked the patient about the daily medication and found no problem. Later, it was discovered that the original patient liked to eat grapefruit, and a few days before the onset of illness, his friend sent a box of grapefruit. He took two or three meals a day and ate for three days. The doctor advised him not to rush to adjust the drug. Try stopping grapefruit first. Three or four days later, the symptoms of hypotension improved.

Zhou Quan said that the current literature reported that the antihypertensive agents that have a significant interaction with grapefruit juice are mainly dihydropyridine calcium antagonists (commonly known as "land-level drugs"), such as felodipine and nifedipine. Therefore, not all types of antihypertensive drugs can be eaten with grapefruit.

"Why does grapefruit have such a strong adverse reaction? This is because grapefruit contains chemical components naringin, furocoumarins, and flavonoids, which interfere with normal human CYP3A4 and P-glycoprotein levels. jobs."

CYP3A4 is an important metabolizing enzyme in the human body. It is distributed in the liver and small intestine. Once this metabolic enzyme is unable to function, the rate at which the body decomposes drugs will slow down, and the amount of time medicines stay in the body will prolong, leading to blood. The drug concentration in the increase.

P-glycoprotein is a transport protein that blocks the absorption of drugs by the small intestine wall and helps to excrete some drugs outside the intestinal tract. When P-glycoprotein is inhibited, the absorption of the drug will increase, causing excessive drug efficacy, aggravating adverse reactions, and even causing poisoning.

However, there are also examples that cause a significant reduction in efficacy. For example, grapefruit juice can reduce the efficacy of clopidogrel, a drug that prevents myocardial infarction.

Which drugs cannot be eaten with grapefruit at the same time?

At present, it is the season when grapefruit is listed. It should be noted that for some patients who use drugs for a long time, some medicines and grapefruit are eaten together, which will produce drug reactions.

“Yesterday morning, a 70-year-old uncle consulted the doctor. He had chronic myelogenous leukemia and he had to eat nilotinib (a drug for treating leukemia) every day. He especially wanted to eat grapefruit these days, but News on the Internet, worried about adverse reactions after eating. The doctor asked me, like him, in the end you can not eat grapefruit?” Zhou Quan said, nilotinib catabolism mainly through CYP3A4, thanks to The uncle is very meticulous. If you don't ask, eating grapefruit will affect the efficacy of the drug and cause side effects.

Studies have shown that 50%-60% of drugs need to be catabolized by CYP3A4. When eating these drugs, it is necessary to avoid eating grapefruit at the same time. These drugs mainly include hypolipidemic drugs, dihydropyridine antihypertensive drugs (such as nifedipine), some sedative hypnotics (such as midazolam), and immunosuppressants (such as cyclosporine, tacrolimus, glucocorticoids). ), some anti-epileptic drugs (such as carbamazepine) and so on. If hypolipidemic drugs and grapefruit are eaten together, muscle lesions, rhabdomyolysis, and even acute kidney failure may occur. A study has been done abroad to take a cup of simvastatin, a hypolipidemic drug. Grapefruit juice served as a pill, which was equivalent to 13 pills delivered with boiled water, resulting in excessive doses.

Zhou Quan said that in the Second Hospital of Zhejiang Medical University, if the patients need to take these drugs when they leave the hospital, they will receive a “Note on Taking Medications,” which states that they should avoid eating grapefruit or grapefruit juice.

So, if you eat grapefruit or drink grapefruit juice, how long does it take to avoid adverse drug reactions? Zhou Quan said that the half-life of grapefruit juice is about 12 hours, that is, after 12 hours, the effect of grapefruit juice on the human body can be reduced to half. When drinking a 250 ml grapefruit juice, its effect is sufficient for 24 hours.

U.S. Food and Drug Administration reminds drug users three years ago that eating grapefruit is dangerous

As early as February 2012, the US Food and Drug Administration official website published the article "Drugs Who Possess Grapefruit or Grapefruit Juice Risky," reminding those who are taking medication that both fresh grapefruit and grapefruit juice are dangerous foods.

Shiew Mei Huang, director of the Center for Clinical Pharmacology of the US Food and Drug Administration, explained in the article: For certain drugs, grapefruit and grapefruit juice increase the absorption of the drug in the blood and increase the side effects of the drug. Chance.

For example, he said that if you drink a large amount of grapefruit juice while taking cholesterol-lowering drugs, due to the increase in drug concentration, cholesterol-reducing drugs that cannot be absorbed will remain in the body, increasing the risk of liver damage and muscle breakdown. May cause kidney failure.

At the same time, studies have shown that grapefruit also has an opposite effect on the human body - reducing the absorption of certain drugs; because it will destroy the role of transporters in the body - the role of transporters.

"For example, grapefruit can reduce the human body's absorption of fexofenadine hydrochloride by blocking the transporter protein, which is a drug that relieves seasonal allergies. Grapefruit can cause this drug to fail, to be reminded that orange juice And apple juice has a similar effect on this drug, so we have asked the drug's instructions to indicate "can not be taken with the juice."

On November 26, 2012, Canadian researchers published a paper in the Journal of the Canadian Medical Association that more and more drugs were found to be associated with grapefruit juice and cause adverse reactions, which may even lead to serious side effects such as sudden death. The researchers said that 85 drugs have been found to react with grapefruit or grapefruit juice, most of which are commonly used drugs. Such as cholesterol-lowering drugs, antibiotics and calcium channel blockers used to treat high blood pressure. In addition, it also involves immunosuppressive drugs for some anticancer drugs and organ transplant patients.

In February 2005, the British Medicines Administration also issued a warning that patients taking hypolipidemic drugs should not eat grapefruit or drink grapefruit juice during their medication, because grapefruit can double the concentration of statins and cause drug poisoning. .

Oranges, bananas, and unpeeled apples should not be eaten with these drugs

Oranges: Studies have found that orange juice increases the transport of OATP (Organic Anion Transporting Peptide) in the small intestine and liver. If you eat oranges and oranges, taking pravastatin (a hypolipidemic drug) can cause the liver to take drugs. Increased ability and bioavailability may cause muscle soreness, fatigue, and other adverse reactions.

Bananas: The use of bananas and water juice prepared by swallowing levodopa formulations (a Parkinson's disease drug), will inhibit the absorption of levodopa, so Parkinson's patients can not swallow levodopa formulations with freshly squeezed banana juice ( Such as Madouba, Singing), it is not recommended to take pills while eating, so as not to reduce the efficacy.

Apple: Peeled apples contain 0.4 micrograms of vitamin K per 100 grams, and unpeeled apples contain 60 micrograms of vitamin K per 100 grams. For adults receiving warfarin (anticoagulant) treatment, daily intake of vitamin K should be controlled at 65-80 micrograms. Eating unpeeled apples will greatly increase the intake of vitamin K, leading to a decrease in the anticoagulant effect of warfarin and possible thrombosis. (Reporter Yu Yu)

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