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Ebastine is a H 1 antihistamine with low potential for causing drowsiness. It does not penetrate the blood–brain barrier to a significant amount and thus combines an effective block of the H 1 receptor in peripheral tissue with a low incidence of central side effects, i.e. seldom causing sedation or drowsiness. [1] [2] [3]
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
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]
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 .
Diphenhydramine, sold under the brand name Benadryl among others, is an antihistamine and sedative. It is a first-generation H 1-antihistamine and it works by blocking certain effects of histamine, which produces its antihistamine and sedative effects. [11] [2] Diphenhydramine is also a potent anticholinergic. [12]
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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 ]
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