First Generation Sedating Antihistamines

First generation sedating antihistamines
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Histamine is a biologically active substance that potentiates the inflammatory and immune responses of the body, regulates physiological function in the gut, and acts as a neurotransmitter. Drugs that antagonize these effects by blocking or inhibiting histamine receptors H receptors are called antihistamines.



First generation sedating antihistamines
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Sedating antihistamines cause sedation as they are highly lipid soluble and readily cross the blood brain barrier. This sedating activity is sometimes used in managing conditions such as eczema where sleep maybe disturbed due to pruritus.



First generation sedating antihistamines
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H 1- antihistamines, the mainstay of treatment for urticaria, were developed from anticholinergic drugs more than 70 years ago. They act as inverse agonists rather than antagonists of histamine H 1 -receptors which are members of the G-protein family.

First generation sedating antihistamines
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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.



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