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It is a second-generation H1-receptor antagonist antihistamine (like its base molecule triprolidine) and works by blocking histamine H1 receptors. [ 1 ] This non-sedating [ verification needed ] antihistamine is sold under the brand name Benadryl Allergy Relief in the United Kingdom by McNeil Laboratories .
Doxylamine and other first-generation antihistamines are the most widely used sleep medications in the world. [6] Typical side effects of doxylamine (at recommended doses) include dizziness, drowsiness, grogginess, and dry mouth, among others. [7] [4] As an antihistamine, doxylamine is an inverse agonist of the histamine H 1 receptor.
H 1 antagonists, also called H 1 blockers, are a class of medications that block the action of histamine at the H 1 receptor, helping to relieve allergic reactions.Agents where the main therapeutic effect is mediated by negative modulation of histamine receptors are termed antihistamines; other agents may have antihistaminergic action but are not true antihistamines.
Doxepin is a highly potent antihistamine, with this being its strongest activity. [ 49 ] [ 53 ] [ 57 ] [ 8 ] In fact, doxepin has been said to be the most or one of the most potent H 1 receptor antagonists available, with one study finding an in vitro K i of 0.17 nM. [ 37 ]
Loratadine is a tricyclic antihistamine, which acts as a selective inverse agonist of peripheral histamine H 1 receptors. [22] [26] The potency of second generation histamine antagonists is (from strongest to weakest) desloratadine (K i 0.4 nM) > levocetirizine (K i 3 nM) > cetirizine (K i 6 nM) > fexofenadine (K i 10 nM
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