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


Antihistamines


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Antihistamines

Old versus new antihistamines. The old ones make you sleepy and probably cause deaths on the road.

Antihistamine tablets, capsules, or liquid medicines
You have seen that there are two main kinds of antihistamines to take by mouth:

 

  • Older antihistamines, which cause sleepiness
  • Newer antihistamines, which cause little or no sleepiness

     

Our advice is that you should not take the older antihistamines which cause sleepiness, unless your doctor prescribes them because you need a tablet to help you sleep. They may be cheap, but there is clear evidence that they may cause road accidents and hinder learning by children in school. The newer antihistamines work just as well and, at least at normal doses, have no measurable harmful effect on driving or learning. The older antihistamines have these harmful effects even in people who do not notice sleepiness from the tablets.

Even preschool children should not have the older antihistamines in our opinion, again unless there is a specific reason why a doctor prescribes them in order to cause sedation or sleepiness. One reason for doing so is to reduce scratching in children with eczema.



The newer low-sedating antihistamines are at least as effective for hayfever and other conditions. They cost more, but are still on the whole reasonably priced.

Examples of the newer and safer antihistamines

Manufacturers can and do change the ingredients of non-prescription medicines without changing the brand name or informing the medical profession. No doubt they do so because they think you are more likely to part with your money on the basis of a known brand name than because you understand what is in the medication. Because of this, information on these drugs is especially likely to become inaccurate. Please let us know if you find errors.

Official name Trade names OTC?*
acrivastine Semprex, Benadryl Allergy Relief capsules No
cetirizine Zirtec, Zyrtec Yes
desloratadine (NEW 2001) Neoclarityn No
fexofenadine Telfast 120, Telfast 180, Allegra No
loratadine Clarityn, Clarityne, Boots Antihistamine Tablets, Claritin Yes
mizolastine Mizollen, Mistamine No
terfenadine (superseded by fexofenadine) Triludan, Seldane, Aller-eze, Histafen Yes
 

*OTC means some or all medicines in this row can be purchased 'over the counter' in the UK, without a doctor's prescription.

 

All these are good. They differ in a number of ways, such as the size of the tablets, the length of time for which they act, how effective they are, the extent to which they may still have a slight tendency to cause sleepiness (though all are superior to old antihistamines for this) and in side effects and drug interactions as well as price. Your doctor should be able to recommend one. Fexofenadine (Telfast) is a development from terfenadine, its main advantage being an improvement in safety. In fact terfenadine is turned into fexofenadine in the body, so people have been exposed to fexofenadine since terfenadine was introduced about 15 years ago. However, fexofenadine, unlike terfenadine and some of the others, is not yet available without a prescription in the UK.

With so many antihistamines which mostly don't cause significant sleepiness, there is no good reason to take one which makes you sleepy unless you particularly want to be made sleepy. True, the older antihistamines are cheaper. But for most of the day it is important that you should have normal alertness. Drowsiness is a cause of accidents and impaired performance in work and study.

Antihistamine sprays or drops for your nose or eyes

Help in the nose or eyes, where they are applied, and only there. If you have symptoms elsewhere, you will need another treatment for those..

As sprays for the nose they are not as effective as steroid sprays , but some people prefer not to use a steroid, and your doctor may prefer to prescribe a drug which is not a steroid. If you think they may suit you, you could try them.

The newer antihistamine eye drops are more important because steroid drops do cause serious side effects sometimes and doctors rightly do not like to use the admittedly effective steroid eye drops. The antihistamine eye drops are similar to the so-called 'antiallergic' eye drops in effectiveness.

 

Examples of antihistamine nose sprays and eye drops

 

Official name Trade names OTC?*
azelastine nasal spray Rhinolast No
levocabastine nasal spray Livostin No
levocabastine eye drops Livostin No
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