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14-September-2008 18:38:39 - Histamine antagonist Redirected from Antihistamine A histamine antagonist is an agent which serves to inhibit the release or action of histamine. Antihistamine can be used to describe any histamine antagonist, but it is usually reserved for the classical antihistamines that act upon the H1 histamine receptor. Antihistamines are used as treatment for allergies. Allergies are caused by an excessive response of the body to allergens, materials that are sometimes omnipresent, such as the pollen released by grasses and trees. An allergic reaction indicates an excessive release, by the body, of histamines. Contents 1 Clinical: H1- and H2-receptor antagonists 1.1 H1-receptor antagonists 1.2 H2-receptor antagonists 2 Experimental: H3- and H4-receptor antagonists 2.1 H3-receptor antagonists 2.2 H4-receptor antagonists 3 Others 3.1 Inhibitors of histamine release 3.2 Other agents with antihistaminergic activity 4 References 5 External links Clinical: H1- and H2-receptor antagonists H1-receptor antagonists Main article: H1 antagonist In common use, the term antihistamine refers only to H1 antagonists, also known as H1 antihistamines. It has been discovered that these H1-antihistamines are actually inverse agonists at the histamine H1-receptor, rather than antagonists per se.1 Clinically, H1 antagonists are used to treat allergic reactions. Examples: Diphenhydramine Loratadine Desloratadine Meclizine Quetiapine this is a side-effect of a drug usually used as an antipsychotic Fexofenadine Pheniramine Cetirizine H2-receptor antagonists Main article: H2 antagonist H2 antagonists, like H1 antagonists, are also inverse agonists and not true antagonists. H2 histamine receptors are found principally in the parietal cells of the gastric mucosa. H2 antagonists are used to reduce the secretion of gastric acid, treating gastrointestinal conditions including peptic ulcers and gastroesophageal reflux disease. Examples: Cimetidine Famotidine Ranitidine Nizatidine Experimental: H3- and H4-receptor antagonists These are experimental agents and do not yet have a defined clinical use, although a number of drugs are currently in human trials. H3-antagonists have a stimulant and nootropic effect, and are being investigated for the treatment of conditions such as ADHD, Alzheimer's Disease and schizophrenia, while H4-antagonists appear to have an immunomodulatory role and are being investigated as antiinflammatory and analgesic drugs. H3-receptor antagonists Main article: H3 antagonist Examples: A-349,821 ABT-239 Ciproxifan Clobenpropit Thioperamide H4-receptor antagonists Examples: Thioperamide JNJ 7777120 VUF-6002 Others Inhibitors of histamine release These agents mast cell stabilizers appear to stabilize the mast cells to prevent degranulation and mediator release. Examples: Cromoglicate cromolyn Nedocromil Other agents with antihistaminergic activity Many drugs, used for other indications, possess unwanted antihistaminergic activity. These include tricyclic antidepressants and antipsychotics. One drug initially developed as an antipsychotic, but now commonly used for its antihistaminic effect, is promethazine. Large doses of vitamin C are known to alleviate shock by inhibiting deaminizing proteins which release histamine. 2 References ^ Leurs R, Church MK, Taglialatela M 2002. H1-antihistamines: inverse agonism, anti-inflammatory actions and cardiac effects. Clin Exp Allergy 32 4: 489-98. doi:10.1046/j.0954-7894.2002.01314.x. PMID 11972592. ^ Klenner, Frederick R. Observations On the Dose and Administration of Ascorbic Acid.... Section Ascorbic acid to the rescue. External links MeSH Histamine+antagonist v d e Histamine antagonists H1 or non-selective Alkylamines Bepotastine Bamipine Brompheniramine Chlorpheniramine Dexbrompheniramine Dexchlorpheniramine Dimethindene Metron S Pheniramine Pyrrobutamine Talastine Thenaldine Tolpropamine Triprolidine Ethanolamines Aminoalkyl ethers Bietanautine Bromazine/Bromodiphenhydramine Carbinoxamine Chlorphenoxamine Clemastine Diphenylpyraline Diphenhydramine Doxylamine Embramine p-Methyldiphenhydramine Moxastine Orphenadrine Phenyltoloxamine Setastine Ethylenediamines Chloropyramine Chlorothen Histapyrrodine Methafurylene Mepyramine Methapyrilene Pyrilamine Talastine Thenyldiamine Thonzylamine Tripelennamine Pyribenzamine Phenothiazine Tricyclics Ahistan Etymemazine Hydroxyethylpromethazine Isopromethazine Isothipendyl Mequitazine Methdilazine Oxomemazine Promethazine Thiazinamium Other Tricyclics Azatadine Clobenzepam Cyproheptadine Deptropine Isothipendyl Loratadine Piperazine Buclizine Chlorcyclizine Cinnarizine Clocinizine Hydroxyzine Niaprazine Oxatomide Benzhydryl compounds Cyclizine, Meclizine Others including selective, 2nd gen, 3rd gen Antazoline Astemizole Azatadine Azelastine Bepottastine Bamipine Cetoxine Clemizole Clobenztropine Deptropine Desloratadine Dimebon Ebastine Emedastine Epinastine Ketotifen Levocabastine Loratadine Mebhydrolin Mizolastine Phenindamine Pimethixene Pyrrobutamine Rupatadine Thenalidine Tritoqualine Alkylamine Acrivastine Tricyclic Olopatadine Piperazine Levocetirizine, Cetirizine Benzhydryl compounds Fexofenadine, Terfenadine H2 Cimetidine Famotidine Ranitidine Roxatidine Lafutidine Niperotidine Nizatidine H3 A-349,821 ABT-239 BF-2649 Burimamide Ciproxifan Clobenpropit Conessine GSK-189,254 GT-2331 Impentamine Iodophenpropit JNJ 5207852 MK-0249 NNC 38-1049 SCH-79687 Thioperamide VUF-5681 H4 JNJ 7777120 Thioperamide VUF-6002 v d e Receptor agonists, antagonists, and reuptake inhibitors BA/M 5-HT serotonin receptor Serotonin receptor agonist 5-HT4 · Serotonin antagonist 5-HT3 · Serotonin uptake inhibitor SSRI Dopamine receptor Dopamine agonist · Dopamine antagonist · Dopamine reuptake inhibitor Adrenergic receptor Adrenergic agonist Alpha, Beta 1/2 · Adrenergic antagonist Alpha 1/2, Beta · Adrenergic uptake inhibitor Histamine receptor Histamine agonist · Histamine antagonist H1, H2, H3 AA GABA receptor GABA agonist · GABA antagonist Glutamate receptor NMDA receptor NMDA receptor antagonist · AMPA receptor Ampakine · Excitatory amino acid agonist · Excitatory amino acid antagonist ANS Acetylcholine receptor Cholinergic Muscarinic, Nicotinic · Anticholinergic Muscarinic, Nicotinic/Ganglionic blocker/Neuromuscular-blocking drugs · Acetylcholinesterase inhibitor Adrenergic receptor SANS only-see above for details PANS Parasympathomimetic Cholinergic, Acetylcholinesterase inhibitor · Parasympatholytic Anticholinergic, Ganglionic blocker SANS Sympathomimetic Adrenergic agonist, Monoamine oxidase inhibitor · Sympatholytic Adrenergic antagonist, Alpha blocker, Ganglionic blocker Retrieved from http://en..org/wiki/Histamine_antagonist Categories: Antihistamines Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Deutsch Español 한국어 This page was last modified on 31 August 2008, at 11:49
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