histamine receptor antagonist

関

specific agents

WordNet

1. a drug that neutralizes or counteracts the effects of another drug
2. a muscle that relaxes while another contracts; "when bending the elbow the triceps are the antagonist"
3. amine formed from histidine that stimulates gastric secretions and dilates blood vessels; released by the human immune system during allergic reactions
4. a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response

PrepTutorEJDIC

1. 対立する人,敵対者,競争相手(opponent)
2. ヒスタミン(子宮収縮・血圧降下の薬)
3. =sense organ / 受信装置

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/10/19 09:10:21」(JST)

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A histamine antagonist (commonly called an antihistamine) is a pharmaceutical drug that inhibits the action of histamine by blocking it from attaching to histamine receptors; or it may inhibit the enzymatic activity of histidine decarboxylase, catalyzing the transformation of histidine into histamine (atypical antihistaminics).

Antihistamines are commonly used for the relief of allergies caused by intolerance of proteins.

Clinical effects

Histamines produce increased vascular permeability, causing fluid to escape from capillaries into tissues, which leads to the classic symptoms of an allergic reaction — a runny nose and watery eyes. Histamine also promotes angiogenesis.

Antihistamines suppress the histamine-induced wheal response (swelling) and flare response (vasodilation) by blocking the binding of histamine to its receptors on nerves, vascular smooth muscle, glandular cells, endothelium, and mast cells. They exert a competitive antagonism to histamines.

Itching and sneezing are suppressed by antihistamine blocking of H1-receptors on nasal sensory nerves.

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. Clinically, H₁ antagonists are used to treat allergic reactions. Sedation is a common side-effect, and some H₁ antagonists, such as diphenhydramine and doxylamine, are also used to treat insomnia. However, second-generation antihistamines do not cross the blood–brain barrier, and as such do not cause drowsiness.

Examples:

• Azelastine
• Brompheniramine
• Buclizine
• Bromodiphenhydramine
• Carbinoxamine
• Cetirizine
• Chlorpromazine (antipsychotic)
• Cyclizine
• Chlorpheniramine
• Chlorodiphenhydramine
• Clemastine
• Cyproheptadine
• Desloratadine
• Dexbrompheniramine
• Deschlorpheniramine
• Dexchlorpheniramine
• Dimenhydrinate (most commonly used as an antiemetic)
• Dimetindene
• Diphenhydramine (Benadryl)
• Doxylamine (most commonly used as an OTC sedative)
• Ebastine
• Embramine
• Fexofenadine
• Levocetirizine
• Loratadine
• Meclozine (most commonly used as an antiemetic)
• Mirtazapine (primarily used to treat depression, also has antiemetic and appetite-stimulating effects)
• Olopatadine (used locally)
• Orphenadrine (a close relative of diphenhydramine used mainly as a skeletal muscle relaxant and anti-Parkinsons agent)
• Phenindamine
• Pheniramine
• Phenyltoloxamine
• Promethazine
• Pyrilamine
• Quetiapine (antipsychotic)
• Rupatadine
• Tripelennamine
• Triprolidine

H₂-receptor antagonists

Main article: H₂ antagonist

H₂ antagonists, like H₁ antagonists, are also inverse agonists and not true antagonists. H₂ histamine receptors, found principally in the parietal cells of the gastric mucosa, are used to reduce the secretion of gastric acid, treating gastrointestinal conditions including peptic ulcers and gastroesophageal reflux disease.

Examples:

• Cimetidine
• Famotidine
• Lafutidine
• Nizatidine
• Ranitidine
• Roxatidine

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, whereas H₄-antagonists appear to have an immunomodulatory role and are being investigated as anti-inflammatory and analgesic drugs.

H₃-receptor antagonists

Main article: H₃ antagonist

Examples:

• A-349,821
• ABT-239
• Ciproxifan
• Clobenpropit
• Conessine
• Thioperamide

H₄-receptor antagonists

Examples:

• Thioperamide
• JNJ 7777120
• VUF-6002

Others

Atypical antihistaminics

They inhibit the enzymatic activity of histidine decarboxylase :

• tritoqualine
• catechin

Mast cell stabilizers

Main article: Mast cell stabilizer

Mast cell stabilizers appear to stabilize the mast cells to prevent degranulation and mediator release. These drugs are not usually classified as histamine antagonists, but have similar indications.

Examples:

• Cromoglicate (cromolyn)
• Nedocromil
• Beta 2 (β2) adrenergic agonists

Other agents with antihistaminergic activity

Many drugs used for other indications possess unwanted antihistaminergic activity.^{[citation needed]}

References

External links

• Histamine+antagonist at the US National Library of Medicine Medical Subject Headings (MeSH)

UpToDate Contents

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English Journal

• Serotonin toxicity in aripiprazole augmentation.

• Primeau M, Pomeraniec F, Wallace DM.
• The Journal of neuropsychiatry and clinical neurosciences.J Neuropsychiatry Clin Neurosci.2012 Dec 1;24(1):E36-7.
• PMID 22450642

• H(1)-histamine receptors in the amygdala are involved in emotional memory but do not mediate anxiety-related behaviors in mice submitted to EPM testing.

• Serafim KR, Gianlorenço AC, Daher FP, Mattioli R.SourceLaboratory of Neuroscience, Physiotherapy Department, Center of Biological Sciences and Health, Federal University of Sao Carlos, Rod. Washington Luis, Km 235, 13565-905 Sao Carlos, Brazil.
• Brain research bulletin.Brain Res Bull.2012 Oct 1;89(1-2):1-7. Epub 2012 Jul 6.
• This study investigated the role of amygdala H(1) receptors in state-dependent memory deficits induced by l-histidine (LH). Tests using an elevated plus-maze (EPM) were performed on two consecutive days: Trial 1 (T1) and Trial 2 (T2). Before each trial, mice were intraperitoneally (IP) injected with
• PMID 22772356

Japanese Journal

• The Role of Histamine H1 and H4 Receptors in Atopic Dermatitis: From Basic Research to Clinical Study

• ,
• Allergology International 63(4), 533-542, 2014
• … Histamine plays important roles in inflammation and nervous irritability in allergic disorders, including atopic dermatitis (AD). … It has been shown to regulate the expression of pruritic factors, such as nerve growth factor and semaphorin 3A, in skin keratinocytes via histamine H1 receptor (H1R). … Furthermore, H1R antagonist reduced the level of IL-31, a cytokine involving the skin barrier and pruritus, in chronic dermatitis lesions in NC/Nga mice and patients with AD. …
• NAID 130004705221

• P7-004　　Histamine inhibits differentiation of skin fibroblasts into myofibroblasts

• 林 琳,澤向 範文,山形 熏,山岡 邦宏,中野 和久,中山田 真吾,田中 良哉
• 日本臨床免疫学会会誌 37(4), 362b-362b, 2014
• … 【Background】Histamine (HA) and TGF-β, major mediators secreted by mast cells are involved in skin inflammation and systemic sclerosis. … 【Methods】Skin fibroblasts (SFBs) were stimulated with TGF-β, HA, or HA receptor antagonists. … 【Results】Expression of H1-receptor (H1R) and H2-receptor (H2R) were detectable in SFBs at both mRNA and protein level. …
• NAID 130004694292

• 緊急消化管内視鏡検査を要した血液透析症例:—当院における過去6年間の臨床的検討—

• 宮澤 晴久,大河原 晋,伊藤 聖学 [他],植田 裕一郎,賀来 佳男,平井 啓之,星野 太郎,名畑 あおい,森 穂波,吉田 泉,宮谷 博幸,吉田 行雄,田部井 薫
• 日本透析医学会雑誌 47(6), 351-357, 2014
• 【目的】当院で緊急消化管内視鏡検査を要した症例をretrospectiveに集計し臨床的背景を明らかにすること. 【対象と方法】対象は2005年1月から2010年12月までの6年間に消化管出血もしくはその疑いのために当院で緊急消化管内視鏡検査を施行した維持血液透析 (HD) 症例44例. 各症例で緊急消化管内視鏡検査施行前後の臨床経過について解析を行った. 【結果】緊急内視鏡検査は重複例を含めて, …
• NAID 130004542537

Related Links

• histamine receptor antagonists - definition of histamine ...

histamine receptor antagonists H 1 receptor antagonist, H 2 receptor antagonist Therapeutics A family of agents that counter histamine activity, which are used to treat conditions linked to ↑ histamine release–eg, mast cell disease ...

• Histamine antagonist

Histamine antagonist A histamine antagonist is an agent that inhibits action of histamine via histamine receptors. H 1 antihistamines are used as treatment for symptoms of allergies such as runny nose. Allergies are caused by an ...

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