Saturday, 9 March 2013

Deadly Combination with Grapefruit:

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grapefruit and deadly combination
It has long been known that grapefruit with certain medications dangerous reactions. Today, however, doctors argue that the risks are greater than previously thought. The combination can lead to an acute renal failure, respiratory failure, stomach and intestinal bleeding, niertoxiteit and even to death.
The reaction takes place because of an active substance in the fruit (called furocoumarinen) the activation of an enzyme in the body stops, which allows for the degradation of drugs. This can ensure that the body perceives as multiple doses of the medication, when in reality you have taken only one dose.


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Structure of histamine
According to scientists, there are more than 85 drugs that can interact with grapefruit, with 43, which can lead to serious side effects. These include statins, immunosuppressive agents( involves an act that reduces the activation or efficacy of the immune system), and antihistamines(produce increased vascular permeability, causing fluid to escape from capillaries into tissues, which leads to the classic symptoms of an allergic reaction — a runny nose and watery eyes).
"Many of the medications that react with grapefruit are frequently prescribed by doctors and are essential for the treatment of common diseases," says the Canadian scientist Dr. David Bailey.
"Recently, we have seen a disturbing trend. Between 2008 and 2012, namely the number of responding medications increased from 17 to 43 percent, which equates to an average increase of six drugs per year. This is due to the introduction of new chemical entities and formulas, "said Dr. Bailey.
A major problem is that many doctors are not aware of the dangers of grapefruit. "And it is only when they know the dangers that they are the cause of the side effects may uncover," says Bailey. "In addition, patients are also unaware of the dangers. It is mainly a lack of knowledge affect us adversely."

What medications?

It is therefore good to know which products you should watch. In the first place, for grapefruit, of course, but also for other citrus fruits, such as the sour orange. Which also contains the furocoumarinen, that the operation of the metabolizing enzyme CYP3A4 counters. This enzyme inactivates in normal cases the effects of some 50 percent of all drugs.
Medications that respond to these chemicals have three characteristics: 1. they can be taken orally, 2. they have a very low to moderate bioavailability (the extent to which the active ingredient becomes available at the intended place) and 3. they undergo metabolism in the gastrointestinal tract through the CYP3A4 enzyme.
In medication with a very low bioavailability, the intake of a normal amount of grapefruit are analogous to multiple doses of the drug alone. The interaction may occur even if the grapefruit many hours for the medication absorbed into the body.
A frequent daily consumption may be a contributory factor. For example, the combination of simvastatin (a statin frequently used) and for three days a glass of grapefruit juice 200 ml, caused a systemic concentration of 330 percent compared to water.

Forty-Five and Older:

The biggest risk is that of the over-45s. They are the most likely to grapefruit to buy and use the most pills.
Due to the size of this population, it is possible that the numerical exposure to the interaction will increase. Especially when you know that older adults are less excessive systemic concentrations of a drug can tolerate. That makes him vulnerable to the interactions.
"This increase makes it necessary to better understand the interactions with grapefruit," says Dr. Bailey. Someone who is happy to play it safe, so better avoid the grapefruit in combination with medication.


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