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H1-antihistamines are further split into three groups known as the first-generation, second-generation and third-generation antihistamines. Another type of antihistamines known as H2-antihistamines are used to treat gastrointestinal conditions caused by excessive stomach acid. [8] Mechanism
The introduction of the first-generation antihistamines marked the beginning of medical treatment of nasal allergies. [28] Research into these drugs led to the discovery that they were H 1 receptor antagonists and also to the development of H 2 receptor antagonists , where H 1 -antihistamines affected the nose and the H 2 -antihistamines ...
The newer, second-generation H 1-antihistamines are far more selective for peripheral histamine H 1-receptors and have a better tolerability profile compared to the first-generation agents. The most common adverse effects noted for second-generation agents include drowsiness, fatigue, headache, nausea and dry mouth. [4]
Like Zyrtec, this is a second-generation antihistamine. “The second generation drugs do not pass as readily into the brain and are less sedating,” Dr. Alan says. NoDerog - Getty Images
An H 3 receptor antagonist is a type of antihistaminic drug used to block the action of histamine at H 3 receptors.. Unlike the H 1 and H 2 receptors which have primarily peripheral actions, but cause sedation if they are blocked in the brain, H 3 receptors are primarily found in the brain and are inhibitory autoreceptors located on histaminergic nerve terminals, which modulate the release of ...
Hydroxyzine, sold under the brand names Atarax and Vistaril among others, is an antihistamine medication. [8] It is used in the treatment of itchiness, anxiety, insomnia, and nausea (including that due to motion sickness). [8] It is used either by mouth or injection into a muscle. [8] Hydroxyzine works by blocking the effects of histamine. [9]
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
Carbinoxamine is an antihistamine and anticholinergic agent. It is used for hay fever, vasomotor rhinitis, mild urticaria, angioedema, dermatographism and allergic conjunctivitis. Carbinoxamine is a histamine antagonist, specifically an H1-antagonist. The maleic acid salt of the levorotatory isomer is sold as the prescription drug rotoxamine.
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