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Mechanism of Action of Antihistamines - Pharmacology V

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e. Anaphylactic Shock. Anaphylactic shock is the most serious type of allergic
reaction. The antigen that produces the response can range from a bee sting toxin to
an antibiotic. Again, this response is produced by an antigen-antibody reaction
characterized by the sudden overwhelming release of histamine in the body. Therefore,
one would expect the effects of histamine on the body to be demonstrated. Two main
effects of anaphylactic shock on the body are severe drops in blood pressure and
impaired respiration. The drastic drop in blood pressure develops from the severe
peripheral vasodilation and the increased permeability of the capillaries. The impaired
breathing arises from bronchoconstriction. The anaphylactic reaction occurs very
rapidly after the introduction of the antigen into the patient. Unless prompt action is
taken by medically trained personnel, the patient will die in a matter of minutes.
f. Prevention or Control of Symptoms of Allergic Reactions. It is possible
to decrease or even prevent the symptoms of an allergic reaction. For a very severe
allergic reaction like anaphylactic shock, a drug that will stop the effects of histamine on
the body must be used. Moreover, the drug must produce positive physiological effects
on the body. The drug used for anaphylactic shock is epinephrine.
g. Desensitization. In some instances, it may be advantageous to prevent an
allergic reaction from occurring. Since the production of abnormal antibodies by the
plasma cells is the real beginning of the potential allergic reaction, it makes sense that if
the abnormal antibodies were not produced, a reaction would not occur when the
antigen again enters the body. The answer would then be to have only complete
(divalent) antibodies produced in the body. This is the basis of treatment to prevent an
allergic reaction. The treatment is referred to as desensitization. Here, extracts of
substances such as pollen or drugs are given to the patient in small, but increasing
doses. In time, the body produces complete antibodies, and the allergic reaction does
not occur.
4-6.
MECHANISM OF ACTION OF ANTIHISTAMINES
a. Antihistamines are drugs that compete with histamines for their receptor sites,
known as H1 and H2 receptor sites. These receptor sites are found in tissue cells, with
H1 receptors located throughout the body and H2 receptor sites found in the gastric
mucosa. The majority of available antihistamines are H1 antagonists.
b. H1 antagonists are believed to act not by opposing but by preventing the
physiologic action of histamine. This occurs because anti-histamine molecules are
chemically similar to histamine molecules. When the antihistamine binds itself to the H1
receptor site, it prevents histamine from doing the same, which effectively eliminates
histamine action.
MD0808
4-6



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