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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 ...
Ball-and-stick model of cimetidine, the prototypical H 2 receptor antagonist. H 2 antagonists, sometimes referred to as H2RAs [1] and also called H 2 blockers, are a class of medications that block the action of histamine at the histamine H 2 receptors of the parietal cells in the stomach. This decreases the production of stomach acid.
A study from 2019 showed that PPI use alone and together with histamine H2-receptor antagonists was associated with an increased bone fracture hazard, which was amplified by days of use and earlier initiation of therapy. [38] The reason is not clear; increased bone break down by osteoclasts has been suggested. [39]
Drug interactions can be of three kinds: additive (the result is what you expect when you add together the effect of each drug taken independently), synergistic (combining the drugs leads to a larger effect than expected), or; antagonistic (combining the drugs leads to a smaller effect than expected). [3]
The action of drugs on the human body (or any other organism's body) is called pharmacodynamics, and the body's response to drugs is called pharmacokinetics. The drugs that enter an individual tend to stimulate certain receptors, ion channels, act on enzymes or transport proteins. As a result, they cause the human body to react in a specific way.
The H 1 receptor is a histamine receptor belonging to the family of rhodopsin-like G-protein-coupled receptors.This receptor is activated by the biogenic amine histamine.It is expressed in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system.
It acts primarily as a strong antagonist of the H 1 receptor (antihistamine, K i = 1.4 nM [29]) and a moderate mACh receptor antagonist (anticholinergic), [2] and also has weak to moderate affinity for the 5-HT 2A, [30] 5-HT 2C, [30] D 2, [31] [32] and α 1-adrenergic receptors, [33] where it acts as an antagonist at all sites, as well.
Mirtazapine is a very strong H 1 receptor antagonist and, as a result, it can cause powerful sedative and hypnotic effects. [11] A single 15 mg dose of mirtazapine to healthy volunteers has been found to result in over 80% occupancy of the H 1 receptor and to induce intense sleepiness . [ 92 ]