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Why Mixing Grapefruit and Prescription Drugs Can Be a Bad Idea

Why Mixing Grapefruit and Prescription Drugs Can Be a Bad Idea



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Check with your pharmacist to see if the drugs you take react badly with this popular citrus fruit

Grapefruit is delicious, but this seemingly harmless fruit can have dangerous side effects when mixed with certain prescription drugs.

Grapefruit is a delicious, versatile citrus fruit, but this seemingly harmless fruit can have dangerous side effects when mixed with certain prescription drugs. More than 85 different drugs have potentially bad reactions with grapefruit, and 43 of those reactions are potentially fatal.

Why is grapefruit part of such a dangerous chemical cocktail? Shiew Mei Huang, acting director of the Food and Drug Administration, explains that, “The juice increases the absorption of the drugs into the bloodstream. When there is a higher concentration of the drug, you tend to have more adverse events." This reaction is caused by chemical compounds called bergamottin and 6', 7'-dihydroxybergamottin, which lessen the ability of enzymes to break down the drugs in the body, possibly causing blood levels of the drug to rise to a dangerous level. In some cases, absorption of the drug is blocked altogether, rendering it useless.

To make the problem more complex, the amount of the enzyme targeted by grapefruit varies in each person, meaning that grapefruit affects different drugs and different people in different ways. The juice of limes, Seville oranges, and even apples can sometimes have similar effects, but they are usually less drastic than those caused by grapefruit.

Among the drugs with which grapefruit should be avoided are Zocor, Lipitor, Pravachol, Viagra and Cialis, Xanax, Valium, Halcion, Cordarone, Multaq, and Nexterone. This is far from a complete list. Consumers are advised to consult their pharmacists or physicians to see if any drugs they take might react adversely with grapefruit, and to also read the medication guide or information sheet that accompanies their prescriptions.


Grapefruit–drug interactions

Some fruit juices and fruits can interact with numerous drugs, in many cases causing adverse effects. [1] The effect was first discovered accidentally, when a test of drug interactions with alcohol used grapefruit juice to hide the taste of the ethanol. [2]

The effect is most studied with grapefruit and grapefruit juice, [1] but similar effects have been observed with certain other citrus fruits. [1] [3] [4] [5] A 2005 medical review advised patients to avoid all citrus juices until further research clarifies the risks. [6] It was reported in 2008 that similar effects had been observed with apple juice. [3] [7] [8]

One whole grapefruit, or a small glass (200 mL, 6.8 US fl oz) of grapefruit juice, can cause drug overdose toxicity. [1] Fruit consumed three days before the medicine can still have an effect. [9] The relative risks of different types of citrus fruit have not been systematically studied. [1] Affected drugs typically have an auxiliary label saying "Do not take with grapefruit" on the container, and the interaction is elaborated upon in the package insert. [10] People are also advised to ask their physician or pharmacist about drug interactions. [10]

The effects are caused by furanocoumarins (and, to a lesser extent, flavonoids). [11] These chemicals inhibit key drug metabolizing enzymes, such as cytochrome P450 3A4 (CYP3A4). CYP3A4 is a metabolizing enzyme for almost 50% of drugs, and is found in the liver and small intestinal epithelial cells. [12] As a result, many drugs are affected. Inhibition of enzymes can have two different effects, depending on whether the drug is either

In the first instance, inhibition of drug-metabolizing enzymes results in elevated concentrations of an active drug in the body, which may cause adverse effects. [10] Conversely, if the medication is a prodrug, it needs to be metabolised to be converted to the active drug. Compromising its metabolism lowers concentrations of the active drug, reducing its therapeutic effect, and risking therapeutic failure.

Low drug concentrations can also be caused when the fruit suppresses drug absorption from the intestine. [13]


Grapefruit–drug interactions

Some fruit juices and fruits can interact with numerous drugs, in many cases causing adverse effects. [1] The effect was first discovered accidentally, when a test of drug interactions with alcohol used grapefruit juice to hide the taste of the ethanol. [2]

The effect is most studied with grapefruit and grapefruit juice, [1] but similar effects have been observed with certain other citrus fruits. [1] [3] [4] [5] A 2005 medical review advised patients to avoid all citrus juices until further research clarifies the risks. [6] It was reported in 2008 that similar effects had been observed with apple juice. [3] [7] [8]

One whole grapefruit, or a small glass (200 mL, 6.8 US fl oz) of grapefruit juice, can cause drug overdose toxicity. [1] Fruit consumed three days before the medicine can still have an effect. [9] The relative risks of different types of citrus fruit have not been systematically studied. [1] Affected drugs typically have an auxiliary label saying "Do not take with grapefruit" on the container, and the interaction is elaborated upon in the package insert. [10] People are also advised to ask their physician or pharmacist about drug interactions. [10]

The effects are caused by furanocoumarins (and, to a lesser extent, flavonoids). [11] These chemicals inhibit key drug metabolizing enzymes, such as cytochrome P450 3A4 (CYP3A4). CYP3A4 is a metabolizing enzyme for almost 50% of drugs, and is found in the liver and small intestinal epithelial cells. [12] As a result, many drugs are affected. Inhibition of enzymes can have two different effects, depending on whether the drug is either

In the first instance, inhibition of drug-metabolizing enzymes results in elevated concentrations of an active drug in the body, which may cause adverse effects. [10] Conversely, if the medication is a prodrug, it needs to be metabolised to be converted to the active drug. Compromising its metabolism lowers concentrations of the active drug, reducing its therapeutic effect, and risking therapeutic failure.

Low drug concentrations can also be caused when the fruit suppresses drug absorption from the intestine. [13]


Grapefruit–drug interactions

Some fruit juices and fruits can interact with numerous drugs, in many cases causing adverse effects. [1] The effect was first discovered accidentally, when a test of drug interactions with alcohol used grapefruit juice to hide the taste of the ethanol. [2]

The effect is most studied with grapefruit and grapefruit juice, [1] but similar effects have been observed with certain other citrus fruits. [1] [3] [4] [5] A 2005 medical review advised patients to avoid all citrus juices until further research clarifies the risks. [6] It was reported in 2008 that similar effects had been observed with apple juice. [3] [7] [8]

One whole grapefruit, or a small glass (200 mL, 6.8 US fl oz) of grapefruit juice, can cause drug overdose toxicity. [1] Fruit consumed three days before the medicine can still have an effect. [9] The relative risks of different types of citrus fruit have not been systematically studied. [1] Affected drugs typically have an auxiliary label saying "Do not take with grapefruit" on the container, and the interaction is elaborated upon in the package insert. [10] People are also advised to ask their physician or pharmacist about drug interactions. [10]

The effects are caused by furanocoumarins (and, to a lesser extent, flavonoids). [11] These chemicals inhibit key drug metabolizing enzymes, such as cytochrome P450 3A4 (CYP3A4). CYP3A4 is a metabolizing enzyme for almost 50% of drugs, and is found in the liver and small intestinal epithelial cells. [12] As a result, many drugs are affected. Inhibition of enzymes can have two different effects, depending on whether the drug is either

In the first instance, inhibition of drug-metabolizing enzymes results in elevated concentrations of an active drug in the body, which may cause adverse effects. [10] Conversely, if the medication is a prodrug, it needs to be metabolised to be converted to the active drug. Compromising its metabolism lowers concentrations of the active drug, reducing its therapeutic effect, and risking therapeutic failure.

Low drug concentrations can also be caused when the fruit suppresses drug absorption from the intestine. [13]


Grapefruit–drug interactions

Some fruit juices and fruits can interact with numerous drugs, in many cases causing adverse effects. [1] The effect was first discovered accidentally, when a test of drug interactions with alcohol used grapefruit juice to hide the taste of the ethanol. [2]

The effect is most studied with grapefruit and grapefruit juice, [1] but similar effects have been observed with certain other citrus fruits. [1] [3] [4] [5] A 2005 medical review advised patients to avoid all citrus juices until further research clarifies the risks. [6] It was reported in 2008 that similar effects had been observed with apple juice. [3] [7] [8]

One whole grapefruit, or a small glass (200 mL, 6.8 US fl oz) of grapefruit juice, can cause drug overdose toxicity. [1] Fruit consumed three days before the medicine can still have an effect. [9] The relative risks of different types of citrus fruit have not been systematically studied. [1] Affected drugs typically have an auxiliary label saying "Do not take with grapefruit" on the container, and the interaction is elaborated upon in the package insert. [10] People are also advised to ask their physician or pharmacist about drug interactions. [10]

The effects are caused by furanocoumarins (and, to a lesser extent, flavonoids). [11] These chemicals inhibit key drug metabolizing enzymes, such as cytochrome P450 3A4 (CYP3A4). CYP3A4 is a metabolizing enzyme for almost 50% of drugs, and is found in the liver and small intestinal epithelial cells. [12] As a result, many drugs are affected. Inhibition of enzymes can have two different effects, depending on whether the drug is either

In the first instance, inhibition of drug-metabolizing enzymes results in elevated concentrations of an active drug in the body, which may cause adverse effects. [10] Conversely, if the medication is a prodrug, it needs to be metabolised to be converted to the active drug. Compromising its metabolism lowers concentrations of the active drug, reducing its therapeutic effect, and risking therapeutic failure.

Low drug concentrations can also be caused when the fruit suppresses drug absorption from the intestine. [13]


Grapefruit–drug interactions

Some fruit juices and fruits can interact with numerous drugs, in many cases causing adverse effects. [1] The effect was first discovered accidentally, when a test of drug interactions with alcohol used grapefruit juice to hide the taste of the ethanol. [2]

The effect is most studied with grapefruit and grapefruit juice, [1] but similar effects have been observed with certain other citrus fruits. [1] [3] [4] [5] A 2005 medical review advised patients to avoid all citrus juices until further research clarifies the risks. [6] It was reported in 2008 that similar effects had been observed with apple juice. [3] [7] [8]

One whole grapefruit, or a small glass (200 mL, 6.8 US fl oz) of grapefruit juice, can cause drug overdose toxicity. [1] Fruit consumed three days before the medicine can still have an effect. [9] The relative risks of different types of citrus fruit have not been systematically studied. [1] Affected drugs typically have an auxiliary label saying "Do not take with grapefruit" on the container, and the interaction is elaborated upon in the package insert. [10] People are also advised to ask their physician or pharmacist about drug interactions. [10]

The effects are caused by furanocoumarins (and, to a lesser extent, flavonoids). [11] These chemicals inhibit key drug metabolizing enzymes, such as cytochrome P450 3A4 (CYP3A4). CYP3A4 is a metabolizing enzyme for almost 50% of drugs, and is found in the liver and small intestinal epithelial cells. [12] As a result, many drugs are affected. Inhibition of enzymes can have two different effects, depending on whether the drug is either

In the first instance, inhibition of drug-metabolizing enzymes results in elevated concentrations of an active drug in the body, which may cause adverse effects. [10] Conversely, if the medication is a prodrug, it needs to be metabolised to be converted to the active drug. Compromising its metabolism lowers concentrations of the active drug, reducing its therapeutic effect, and risking therapeutic failure.

Low drug concentrations can also be caused when the fruit suppresses drug absorption from the intestine. [13]


Grapefruit–drug interactions

Some fruit juices and fruits can interact with numerous drugs, in many cases causing adverse effects. [1] The effect was first discovered accidentally, when a test of drug interactions with alcohol used grapefruit juice to hide the taste of the ethanol. [2]

The effect is most studied with grapefruit and grapefruit juice, [1] but similar effects have been observed with certain other citrus fruits. [1] [3] [4] [5] A 2005 medical review advised patients to avoid all citrus juices until further research clarifies the risks. [6] It was reported in 2008 that similar effects had been observed with apple juice. [3] [7] [8]

One whole grapefruit, or a small glass (200 mL, 6.8 US fl oz) of grapefruit juice, can cause drug overdose toxicity. [1] Fruit consumed three days before the medicine can still have an effect. [9] The relative risks of different types of citrus fruit have not been systematically studied. [1] Affected drugs typically have an auxiliary label saying "Do not take with grapefruit" on the container, and the interaction is elaborated upon in the package insert. [10] People are also advised to ask their physician or pharmacist about drug interactions. [10]

The effects are caused by furanocoumarins (and, to a lesser extent, flavonoids). [11] These chemicals inhibit key drug metabolizing enzymes, such as cytochrome P450 3A4 (CYP3A4). CYP3A4 is a metabolizing enzyme for almost 50% of drugs, and is found in the liver and small intestinal epithelial cells. [12] As a result, many drugs are affected. Inhibition of enzymes can have two different effects, depending on whether the drug is either

In the first instance, inhibition of drug-metabolizing enzymes results in elevated concentrations of an active drug in the body, which may cause adverse effects. [10] Conversely, if the medication is a prodrug, it needs to be metabolised to be converted to the active drug. Compromising its metabolism lowers concentrations of the active drug, reducing its therapeutic effect, and risking therapeutic failure.

Low drug concentrations can also be caused when the fruit suppresses drug absorption from the intestine. [13]


Grapefruit–drug interactions

Some fruit juices and fruits can interact with numerous drugs, in many cases causing adverse effects. [1] The effect was first discovered accidentally, when a test of drug interactions with alcohol used grapefruit juice to hide the taste of the ethanol. [2]

The effect is most studied with grapefruit and grapefruit juice, [1] but similar effects have been observed with certain other citrus fruits. [1] [3] [4] [5] A 2005 medical review advised patients to avoid all citrus juices until further research clarifies the risks. [6] It was reported in 2008 that similar effects had been observed with apple juice. [3] [7] [8]

One whole grapefruit, or a small glass (200 mL, 6.8 US fl oz) of grapefruit juice, can cause drug overdose toxicity. [1] Fruit consumed three days before the medicine can still have an effect. [9] The relative risks of different types of citrus fruit have not been systematically studied. [1] Affected drugs typically have an auxiliary label saying "Do not take with grapefruit" on the container, and the interaction is elaborated upon in the package insert. [10] People are also advised to ask their physician or pharmacist about drug interactions. [10]

The effects are caused by furanocoumarins (and, to a lesser extent, flavonoids). [11] These chemicals inhibit key drug metabolizing enzymes, such as cytochrome P450 3A4 (CYP3A4). CYP3A4 is a metabolizing enzyme for almost 50% of drugs, and is found in the liver and small intestinal epithelial cells. [12] As a result, many drugs are affected. Inhibition of enzymes can have two different effects, depending on whether the drug is either

In the first instance, inhibition of drug-metabolizing enzymes results in elevated concentrations of an active drug in the body, which may cause adverse effects. [10] Conversely, if the medication is a prodrug, it needs to be metabolised to be converted to the active drug. Compromising its metabolism lowers concentrations of the active drug, reducing its therapeutic effect, and risking therapeutic failure.

Low drug concentrations can also be caused when the fruit suppresses drug absorption from the intestine. [13]


Grapefruit–drug interactions

Some fruit juices and fruits can interact with numerous drugs, in many cases causing adverse effects. [1] The effect was first discovered accidentally, when a test of drug interactions with alcohol used grapefruit juice to hide the taste of the ethanol. [2]

The effect is most studied with grapefruit and grapefruit juice, [1] but similar effects have been observed with certain other citrus fruits. [1] [3] [4] [5] A 2005 medical review advised patients to avoid all citrus juices until further research clarifies the risks. [6] It was reported in 2008 that similar effects had been observed with apple juice. [3] [7] [8]

One whole grapefruit, or a small glass (200 mL, 6.8 US fl oz) of grapefruit juice, can cause drug overdose toxicity. [1] Fruit consumed three days before the medicine can still have an effect. [9] The relative risks of different types of citrus fruit have not been systematically studied. [1] Affected drugs typically have an auxiliary label saying "Do not take with grapefruit" on the container, and the interaction is elaborated upon in the package insert. [10] People are also advised to ask their physician or pharmacist about drug interactions. [10]

The effects are caused by furanocoumarins (and, to a lesser extent, flavonoids). [11] These chemicals inhibit key drug metabolizing enzymes, such as cytochrome P450 3A4 (CYP3A4). CYP3A4 is a metabolizing enzyme for almost 50% of drugs, and is found in the liver and small intestinal epithelial cells. [12] As a result, many drugs are affected. Inhibition of enzymes can have two different effects, depending on whether the drug is either

In the first instance, inhibition of drug-metabolizing enzymes results in elevated concentrations of an active drug in the body, which may cause adverse effects. [10] Conversely, if the medication is a prodrug, it needs to be metabolised to be converted to the active drug. Compromising its metabolism lowers concentrations of the active drug, reducing its therapeutic effect, and risking therapeutic failure.

Low drug concentrations can also be caused when the fruit suppresses drug absorption from the intestine. [13]


Grapefruit–drug interactions

Some fruit juices and fruits can interact with numerous drugs, in many cases causing adverse effects. [1] The effect was first discovered accidentally, when a test of drug interactions with alcohol used grapefruit juice to hide the taste of the ethanol. [2]

The effect is most studied with grapefruit and grapefruit juice, [1] but similar effects have been observed with certain other citrus fruits. [1] [3] [4] [5] A 2005 medical review advised patients to avoid all citrus juices until further research clarifies the risks. [6] It was reported in 2008 that similar effects had been observed with apple juice. [3] [7] [8]

One whole grapefruit, or a small glass (200 mL, 6.8 US fl oz) of grapefruit juice, can cause drug overdose toxicity. [1] Fruit consumed three days before the medicine can still have an effect. [9] The relative risks of different types of citrus fruit have not been systematically studied. [1] Affected drugs typically have an auxiliary label saying "Do not take with grapefruit" on the container, and the interaction is elaborated upon in the package insert. [10] People are also advised to ask their physician or pharmacist about drug interactions. [10]

The effects are caused by furanocoumarins (and, to a lesser extent, flavonoids). [11] These chemicals inhibit key drug metabolizing enzymes, such as cytochrome P450 3A4 (CYP3A4). CYP3A4 is a metabolizing enzyme for almost 50% of drugs, and is found in the liver and small intestinal epithelial cells. [12] As a result, many drugs are affected. Inhibition of enzymes can have two different effects, depending on whether the drug is either

In the first instance, inhibition of drug-metabolizing enzymes results in elevated concentrations of an active drug in the body, which may cause adverse effects. [10] Conversely, if the medication is a prodrug, it needs to be metabolised to be converted to the active drug. Compromising its metabolism lowers concentrations of the active drug, reducing its therapeutic effect, and risking therapeutic failure.

Low drug concentrations can also be caused when the fruit suppresses drug absorption from the intestine. [13]


Grapefruit–drug interactions

Some fruit juices and fruits can interact with numerous drugs, in many cases causing adverse effects. [1] The effect was first discovered accidentally, when a test of drug interactions with alcohol used grapefruit juice to hide the taste of the ethanol. [2]

The effect is most studied with grapefruit and grapefruit juice, [1] but similar effects have been observed with certain other citrus fruits. [1] [3] [4] [5] A 2005 medical review advised patients to avoid all citrus juices until further research clarifies the risks. [6] It was reported in 2008 that similar effects had been observed with apple juice. [3] [7] [8]

One whole grapefruit, or a small glass (200 mL, 6.8 US fl oz) of grapefruit juice, can cause drug overdose toxicity. [1] Fruit consumed three days before the medicine can still have an effect. [9] The relative risks of different types of citrus fruit have not been systematically studied. [1] Affected drugs typically have an auxiliary label saying "Do not take with grapefruit" on the container, and the interaction is elaborated upon in the package insert. [10] People are also advised to ask their physician or pharmacist about drug interactions. [10]

The effects are caused by furanocoumarins (and, to a lesser extent, flavonoids). [11] These chemicals inhibit key drug metabolizing enzymes, such as cytochrome P450 3A4 (CYP3A4). CYP3A4 is a metabolizing enzyme for almost 50% of drugs, and is found in the liver and small intestinal epithelial cells. [12] As a result, many drugs are affected. Inhibition of enzymes can have two different effects, depending on whether the drug is either

In the first instance, inhibition of drug-metabolizing enzymes results in elevated concentrations of an active drug in the body, which may cause adverse effects. [10] Conversely, if the medication is a prodrug, it needs to be metabolised to be converted to the active drug. Compromising its metabolism lowers concentrations of the active drug, reducing its therapeutic effect, and risking therapeutic failure.

Low drug concentrations can also be caused when the fruit suppresses drug absorption from the intestine. [13]