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Another type of antihistamines known as H2-antihistamines are used to treat gastrointestinal conditions caused by excessive stomach acid. [8] Mechanism. H-1 antihistamines work by inhibiting histamine from binding to H-1 receptors. Histamine receptors expressed in smooth muscles, vascular endothelial cells, the heart, and the central nervous ...
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 sneezing).
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.
PET studies with antihistamines have found that brain H 1 receptor occupancy of more than 50% is associated with a high prevalence of somnolence and cognitive decline, whereas brain H 1 receptor occupancy of less than 20% is considered to be non-sedative. [46] Hydroxyzine also acts as a functional inhibitor of acid sphingomyelinase. [47]
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.
Loratadine, sold under the brand name Claritin among others, is a medication used to treat allergies. [5] This includes allergic rhinitis (hay fever) and hives. [5] It is also available in drug combinations such as loratadine/pseudoephedrine, in which it is combined with pseudoephedrine, a nasal decongestant. [5]
Tripelennamine, sold under the brand name Pyribenzamine by Novartis, is a drug that is used as an antipruritic and first-generation antihistamine. It can be used in the treatment of asthma, hay fever, rhinitis, and urticaria, but is now less common as it has been replaced by newer antihistamines. The drug was patented at CIBA, which merged with ...
Brompheniramine, sold under the brand name Dimetapp among others, is a first-generation antihistamine drug of the propylamine (alkylamine) class. [2] It is indicated for the treatment of the symptoms of the common cold and allergic rhinitis, such as runny nose, itchy eyes, watery eyes, and sneezing.