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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.
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]
It is classified as a second-generation antihistamine because it is less able to pass the blood–brain barrier and cause sedation, compared to first-generation antihistamines. [12] [13] It was patented in 1979 and came into medical use in 1996. [14] It is on the World Health Organization's List of Essential Medicines. [15]
Itching, sneezing, and inflammatory responses are suppressed by antihistamines that act on H1-receptors. [2] [8] In 2014, antihistamines such as desloratadine were found to be effective to complement standardized treatment of acne due to their anti-inflammatory properties and their ability to suppress sebum production. [9] [10]
Cimetidine was the prototypical histamine H 2 receptor antagonist from which later drugs were developed. Cimetidine was the culmination of a project at Smith, Kline & French (SK&F; now GlaxoSmithKline) by James W. Black, C. Robin Ganellin, and others to develop a histamine receptor antagonist that would suppress stomach acid secretion.
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]
Mebhydrolin or mebhydroline is an antihistamine. It is not available in the United States, but it is in various other countries under the brand names Bexidal ( BD ) and Diazolin ( RU ) . It is used for symptomatic relief of allergic symptoms caused by histamine release, including nasal allergies and allergic dermatosis.
A histamine agonist is a drug which causes increased activity at one or more of the four histamine receptor subtypes. H 1 agonists promote wakefulness. [1] H 2: Betazole and Impromidine are examples of agonists used in diagnostics to increase histamine. H 3: Betahistine is a weak Histamine 1 agonist and a very strong antagonist of the Histamine ...