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Histamine antagonistA histamine antagonist is an agent which serves to inhibit the release or action of histamine. Although the term "antihistamine" could technically be used for any histamine antagonist, in practice the term is reserved for the classical antihistamines which act upon the H1 histamine receptor. Additional recommended knowledge
Clinical: H1- and H2-receptor antagonistsH1-receptor antagonistsIn common use, the term antihistamine refers only to H1-receptor antagonists, also known as H1-antihistamines. It has been discovered that these H1-antihistamines are actually inverse agonists at the histamine H1-receptor, rather than antagonists per se. [1] H2-receptor antagonistsClinically-relevant histamine H2-receptors are found principally in the parietal cells of the gastric mucosa. H2-receptor "antagonists" are also inverse agonists, rather than true antagonists; and are used to reduce the secretion of gastric acid. Examples include cimetidine, ranitidine, and famotidine. Experimental: H3- and H4-receptor antagonistsThese are experimental agents and do not yet have a defined clinical use. H3-receptor antagonists
H4-receptor antagonists
OthersInhibitors of histamine releaseThese agents (mast cell stabilizers) appear to stabilise the mast cells to prevent degranulation and mediator release.
Other agents with antihistaminergic activityMany drugs, used for other indications, possess unwanted antihistaminergic activity. These include tricyclic antidepressants, antipsychotics, etc. References
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This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Histamine_antagonist". A list of authors is available in Wikipedia. |