Everything about Anti-histamine totally explained
A
histamine antagonist is an agent which serves to inhibit the release or action of
histamine.
Antihistamine can be used to describe any histamine antagonist, but it's usually reserved for the
classical antihistamines that act upon the
H1 histamine receptor.
Clinical: H1- and H2-receptor antagonists
H1-receptor antagonists
In common use, the term antihistamine refers only to H
1 antagonists, also known as H
1 antihistamines. It has been discovered that these H
1-antihistamines are actually
inverse agonists at the histamine H
1-receptor, rather than
antagonists per se. Clinically, H
1 antagonists are used to treat
allergic reactions.
Examples:
H2-receptor antagonists
H
2 antagonists, like H
1 antagonists, are also
inverse agonists and not true
antagonists. H
2 histamine receptors are found principally in the
parietal cells of the
gastric mucosa. H
2 antagonists are used to reduce the secretion of
gastric acid, treating
gastrointestinal conditions including
peptic ulcers and
gastroesophageal reflux disease.
Examples:
Cimetidine
Famotidine
Ranitidine
Experimental: H3- and H4-receptor antagonists
These are experimental agents and don't yet have a defined clinical use.
H3-receptor antagonists
Examples:
ABT-239
Cipralisant
Ciproxifan
Clobenpropit
Thioperamide
H4-receptor antagonists
Examples:
Thioperamide
Others
Inhibitors of histamine release
These agents (mast cell stabilizers) appear to stabilize the mast cells to prevent degranulation and mediator release.
Examples:
Cromoglicate (cromolyn)
Nedocromil
Other agents with antihistaminergic activity
Many drugs, used for other indications, possess unwanted antihistaminergic activity. These include tricyclic antidepressants and antipsychotics.
Large doses of vitamin C are known to alleviate shock by inhibiting deaminizing proteins which release histamine.
Further Information
Get more info on 'Anti-histamine'.
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