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H 1-receptor antagonists are competitive inhibitor of histamine receptor H 1 and are used to treat allergies. This group is often referred simply as antihistamines . Wikimedia Commons has media related to H1 receptor antagonists .
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.
Rupatadine is a second generation, non-sedating, long-acting histamine antagonist with selective peripheral H 1 receptor antagonist activity. It further blocks the receptors of the platelet-activating factor (PAF) according to in vitro and in vivo studies.
H 1-antihistamines work by binding to histamine H 1 receptors in mast cells, smooth muscle, and endothelium in the body as well as in the tuberomammillary nucleus in the brain. Antihistamines that target the histamine H 1-receptor are used to treat allergic reactions in the nose (e.g., itching, runny nose, and
Histamine receptors expressed in smooth muscles, vascular endothelial cells, the heart, and the central nervous system. [7] This prevents a range of cellular signaling cascades that lead to vasodilation and increased membrane permeability from happening, thus preventing allergic symptoms.
Histaminergic means "working on the histamine system", and histaminic means "related to histamine". [1] A histaminergic agent (or drug) is a chemical which functions to directly modulate the histamine system in the body or brain. Examples include histamine receptor agonists and histamine receptor antagonists (or antihistamines).
[medical citation needed] Loratadine is a long-acting antihistamine (H 1 histamine antagonist) that is less sedating than older substances of its type. [medical citation needed] In 2022, it was the 289th most commonly prescribed medication in the United States, with more than 500,000 prescriptions. [2] [3]
Clemastine, also known as meclastin, is a first-generation H1 histamine antagonist (antihistamine) with anticholinergic properties (drying) and sedative side effects. [1] Like all first-generation antihistamines, it is sedating. [2] [3] Patented in 1960, it came into medical use in 1967. [4]