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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 ...
Fexofenadine, sold under the brand name Allegra among others, [10] is an antihistamine pharmaceutical drug used in the treatment of allergy symptoms, such as hay fever and urticaria. [11] Therapeutically, fexofenadine is a selective peripheral H 1 blocker.
It contains fexofenadine, as the hydrochloride, an antihistamine; and pseudoephedrine, as the hydrochloride, a nasal decongestant. [ 2 ] In 2021, it was the 279th most commonly prescribed medication in the United States, with more than 800,000 prescriptions.
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.
[1] [2] Histamine receptors are proteins that bind with histamine, a neurotransmitter involved in various physiological processes. There are four main types: H1, H2, H3, and H4. H1 receptors are linked to allergic responses, H2 to gastric acid regulation, H3 to neurotransmitter release modulation, and H4 to immune system function.
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.
Terfenadine acts as a peripherally-selective antihistamine, or antagonist of the histamine H 1 receptor. [3] It is a prodrug, generally completely metabolized to the active form fexofenadine in the liver by the enzyme cytochrome P450 3A4. Due to its near complete metabolism by the liver immediately after leaving the gut, terfenadine normally is ...
In addition, subjective sleepiness correlated well with the brain H 1 receptor occupancy. [45] 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 ...