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Home » GATE Study Material » Pharmaceutical Science » Medicinal Chemistry » Antihistamines


Antihistamines


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Antihistamines

Are antihistamines safe?

All medicines have side effects, but some have very few, mostly mild, whilst others have a lot, mostly serious.

The latest antihistamines are amongst the safest medicines there are. But there are differences between them in side effects.



 

Older antihistamines are bad news unless you need help getting to sleep

Older antihistamines do have more side effects. The most serious of these are both sleepiness, and a harmful effect on driving, learning and similar tasks even when they don't seem to make you feel sleepy. They affect your brain in the same way as alcohol.

There is no real doubt in the minds of researchers that older antihistamines can cause road accidents.

They also hinder learning, exam performance and skilled tasks.

Older antihistamines also had some other side effects which might in a few people cause difficulty passing water or increased pressure in the eyes (glaucoma), although this seems to have been rare.

There is now little reason to use the older antihistamines.

How do we know that the new antihistamines are better? There has been lots of research which shows this, but two experiments are specially interesting.

Road safety experiment

In one set of experiments, drivers had to drive along a motorway for 100 kilometres. They had to drive at a steady speed and keep as near to the middle of the slowest lane (the left hand lane, as it was in the Netherlands) as they could. A video camera on the roof of the car filmed the white line on the road. When they got back, the video tape was played, and the movement of the white line on the screen was measured.

In some tests the drivers took an old antihistamine, and in other tests they took a new one or a dummy tablet.

The old antihistamines made the drivers wobble more during driving, sometimes to a dangerous extent, so that the test drive had to be stopped. (They used dual control cars, and had permission to stop on the hard shoulder of the road when this happened.) Old antihistamines were frankly dangerous.

New antihistamines caused no increase in wobbling compared to the dummy tablets.

Alcohol, even within the legal limit for driving, also made steering more wobbly. But the new antihistamines together with alcohol were no worse than the alcohol alone.

So the new antihistamines are much safer for drivers.

Learning experiment in children with hayfever

Schoolchildren with hayfever were divided into three groups. For the experiment, during the hayfever season, children in the first group took dummy tablets. Those in the second group took an old antihistamine. Children in the third group took a new antihistamine, Triludan.

All the children then sat in front of computers. They used a computer program which taught them about farming in the Sahel Desert. As the children were from the town of Maastricht in the Netherlands, this meant they knew nothing about this at the beginning.

When the children had finished learning, they played a computer game. Guess what? The game was about - farming in the Sahel desert. Depending how well they did, each child got a score.

Here are the results. The children whose hayfever was treated with the old antihistamine did WORSE than the ones who just got dummy tablets. The sleepiness, or inattentiveness did more harm to how they did than hayfever alone.

But the children who took the new antihistamine, Triludan, did BETTER than the children who took dummy tablets. This shows that hayfever by itself harms learning, and that treating the hayfever undoes this harm, provided the treatment does not make the children sleepy.

Both sets of experiments were done by the team of Professor O'Hanlon, of Maastricht, Netherlands. If he'd let me use some photographs of these experiments, I would show them to you on the web.

Many other experimens have shown similar results.

So the new antihistamines are much better for schoolchildren, students, and people who need to use their brains, which means all of us.

Two of the newer antihistamines do have a rare but serious problem

Two of the newer antihistamines (terfenadine and astemizole) have on rare occasions had life-threatening or fatal side effects. In overdose or when combined with one of a small number of other medicines, or in people with certain kinds of heart trouble, they could cause the heart to beat in an abnormal way, and over enormous numbers of people who took the drug, a small number of people died. With proper precautions terfenadine and astemizole are still very good and safe drugs. But in the case of terfenadine even that problem has now been solved. In the body, terfenadine is changed into something else which has the good effects of terfenadine but not the bad effects. So the obvious answer was to put the something else into a tablet. This has now been done. The new medicine is called Telfast in Britain (Allegra in the USA), and its official name is fexofenadine. Fexofenadine has the good effects of terfenadine but not its very rare serious side effect.

So the bottom line is: some of the latest antihistamines are among the safest medicines there are. If they relieve a real illness, it is reasonable to take them, if necessary over long periods, without worrying.

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