Antihistaminergic
| Antihistamines | |
|---|---|
| Drug class | |
Histamine structure
|
|
| Class identifiers | |
| ATC code | R06 |
| Mechanism of action | • Receptor antagonist • Inverse agonist |
| Biological target |
Histamine receptors • HRH1 • HRH2 • HRH3 • HRH4 |
| External links | |
| MeSH | D006633 |
An antihistamine is a type of pharmaceutical drug that opposes the activity of histamine receptors in the body. Antihistamines are subclassified according to the histamine receptor that they act upon: the two largest classes of antihistamines are H1-antihistamines and H2-antihistamines. Antihistamines that target the histamine H1-receptor are used to treat allergic reactions in the nose (e.g., itching, runny nose, and sneezing) as well as for insomnia. They are sometimes also used to treat motion sickness or vertigo caused by problems with the inner ear. Antihistamines that target the histamine H2-receptor are used to treat gastric acid conditions (e.g., peptic ulcers and acid reflux). H1-antihistamines work by binding to histamine H1 receptors in mast cells, smooth muscle, and endothelium in the body as well as in the tuberomammillary nucleus in the brain; H2-antihistamines bind to histamine H2 receptors in the upper gastrointestinal tract, primarily in the stomach.
Histamine receptors exhibit constitutive activity, so antihistamines can function as either a neutral receptor antagonist or an inverse agonist at histamine receptor. Only a few currently marketed H1-antihistamines are known to function as inverse agonists.
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