A Brief Overview Of First Generation Antihistamines And Following

For millions of sufferers, allergic reactions to such triggers as grass, pollen, insect bites, animal dander and certain types of foods, make certain seasons a time of sneezing, itching, runny nose and sometimes sinusitis. Histamines are organic nitrogen molecules that are released when the body is fighting off the effects of allergens. Histamines are released from the body’s immune system to help in fighting off the allergen invaders. Histamines help the immune system to be better able to penetrate the foreign elements. This leaves the area where the allergens are found inflamed and swollen. First generation antihistamines help the body to recover from the effects of the release of histamines.

The oldest group of these medications does a good job of alleviating sufferers from the symptoms that mark the release of histamine compounds, but they also make the individual drowsy. Second generation antihistamines and third generation antihistamines followed with fewer side effects such as drowsiness. Second generation antihistamines no longer left the patient feeling sedated. Third generation antihistamines were built on the second generation medications that made them even better. Even those medications that left one feeling sleepy and drugged were able to offer relief from the allergen compounds.

The first antihistamine discovered was piperoxin. It was identified in 1933 by Ernest Fourneau and Daniel Bovet. In 1957, Bovet won the Nobel Prize in Physiology or Medicine for his contribution in the breakthrough. The main classes of early medications are Ethylenediamines, Ethanolamines, Alkylamines, Piperazines, and Tricyclics and Tetracyclics. Typical category products are Diphenhydramine, Dimenhydrinate, Clemastine, Chlorpheniramine and Brompheniramine. The above compounds are a major component of over-the-counter medications such as Benadryl, Tavist, Allerhist, Chlor-Trimeton, Nasahist, Dimetane, Bromphen, Dramamine and Dimetapp. These products are generally available over-the-counter. The prices tend to be inexpensive, and they do relieve allergic symptoms.

First generation antihistamines can cause the user to have dry mouth and eyes. There may be headaches and abdominal pain. The ability to drive or to operate other machines and tools can be compromised. The medication can cause the individual to feel significant drowsiness. With the older classifications, complications can occur if the individual is taking other medications. Examples of unfortunate combinations include sleeping pills, muscle relaxants or sedatives. It is very important to consult with a medical professional before taking these drugs, particularly the first grouping of medications. Avoiding any type of drug combinations when you don’t know the results can be dangerous.

The first of the effective antihistamine medications to be developed was of the class Ethylediamines. Examples of this class of medications include Mepyramine, which is also known as pyrilamine. Another example is Antazoline. Mepyramine causes drowsiness in many users. It is commonly used in remedies for the common cold and as a remedy for some menstrual symptoms. If used as a topical cream, it is helpful in the treatment for insect bites, nettle rash and insect stings. Antazoline often appears as an ingredient in eye drops and in nasal congestion remedies.

Ethanolamines is the next class of antihistamines to be developed. Diphenhydramine is an example of this type of medication. This class of drugs has effects that could be considered significant. Sedation is just one example of negative effects. However, gastrointestinal adverse symptoms don’t happen often in the population of those taking the drugs. In addition to diphenhydramine, other examples from this drug group include dimenhydrinate, clemastine, doxylamine and carbinoxamine. Diphenhydramine is mainly used as an allergy remedy. It is used as a sleep aid and as a help for anxiety disorders. The drug has a strong hypnotic effect. Carbinoxamine is often used in the treatment of hay fever, and related symptoms. It was first marketed under the brand name Clistin. Doxylamine is both a nighttime cold medicine and to prevent morning sickness. Clemastine has fewer side effects than some of the other first level medications. It also stops itching. Dimenhydrinate helps to control motion sickness and nausea. It is marketed in the United States as Dramamine.

Alkylamines are noted for a lower incidence of gastrointestinal and sedative effects, but it has a higher level of central nervous system stimulation. Examples of this class of medications include pheniramine, chlorphenamine, dexchlorpheniramine, brompheniramine, triprolidine and dimetindene. Pheniramine has strong sedation effects, to the point where it is sometimes used as a sleeping aid, over-the-counter. Chlorphenamine is used in small veterinary practices and as a medication, along with dexchlorpheniramine, to control rhinitis and similar symptoms.

Piperazines are the fourth of the classes in the first generation antihistamines. This group is typically used for combating motion sickness, nausea, vomiting and vertigo. This group has significant adverse effects in some areas.

Tricyclics and tetracyclics are the fifth of five classes of the first medication cycle. These medications have slightly different structure than other classes, but still suffer from some of the same types of adverse reactions. There are close links between this class and others of the same classes. Some of the later drugs are built upon the foundation of this class. There may not be improved efficacy, but reducing the negative effects is seen as a move in the right direction.

Second generation antihistamines are designed to limit the sedation effects of the earlier drugs, without sacrificing effectiveness. These and Third generation antihistamines do not cross the blood-brain barrier, making them quite selective in their application. In other words, they treat the allergic reaction without causing sedation or drowsiness. They are also able to avoid stomach problems, involuntary nervous system activities and similar symptoms.

For those who must find relief from allergy symptoms, hay fever symptoms and other complications of pollen, dust mites, hay fever, sinus congestion, rhinitis and similar triggers, first generation antihistamines, second generation antihistamines and third generation antihistamines are a significant boon. Today, these conditions can be managed, day and night by specific medications that address the parts of the body most affected. Not all medical professionals believe that second and third generation drugs are significantly more effective than the first grouping. However, it is apparent that the lack of adverse symptoms is a significant benefit to those forced to take the medications.

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