ロイコトリエン受容体遮断薬、ロイコトリエン受容体拮抗薬

関: leukotriene antagonist

WordNet

a drug that neutralizes or counteracts the effects of another drug
a muscle that relaxes while another contracts; "when bending the elbow the triceps are the antagonist"
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

対立する人,敵対者,競争相手(opponent)
=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）』「2014/04/04 22:41:47」(JST)

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[Wiki en表示]

A leukotriene antagonist (sometimes referred to as a leukast) is a drug that inhibits leukotrienes, which are fatty compounds produced by the immune system that cause inflammation in asthma and bronchitis, and constrict airways.

Leukotriene inhibitors (or modifiers), such as montelukast (trade names Singulair and Montelo-10), zafirlukast, pranlukast and zileuton, are used to treat those diseases. They are less effective than corticosteroids thus less preferred in the treatment of asthma.^[1]

Approaches

There are two main approaches to block the actions of leukotrienes.

Inhibition of the 5-lipoxygenase pathway

Drugs such as zileuton block 5-lipoxygenase, inhibiting the synthetic pathway of leukotriene metabolism, whereas drugs such as MK-886 block the 5-lipoxygenase activating protein (FLAP) and may help in treating atherosclerosis.^[2]

Antagonism of cysteinyl-leukotriene type 1 receptors

Agents such as montelukast and zafirlukast block the actions of cysteinyl leukotrienes at the CysLT1 receptor on target cells such as bronchial smooth muscle.

These modifiers have been shown to improve asthma symptoms, reduce asthma exacerbations and limit markers of inflammation such as eosinophil counts in the peripheral blood and bronchoalveolar lavage fluid. This demonstrates that they have anti-inflammatory properties.

References

^ Fanta CH (March 2009). "Asthma". N Engl J Med 360 (10): 1002–14. doi:10.1056/NEJMra0804579. PMID 19264689.
^ Jawien, J.; Gajda, M.; Rudling, M.; Mateuszuk, L.; Olszanecki, R.; Guzik, T. J.; Cichocki, T.; Chlopicki, S.; Korbut, R. (March 2006). "Inhibition of five lipoxygenase activating protein (FLAP) by MK-886 decreases atherosclerosis in apoE/LDLR-double knockout mice". European Journal of Clinical Investigation 36 (3): 141–146. doi:10.1111/j.1365-2362.2006.01606.x. PMID 16506957.

External links

Leukotriene antagonists at the US National Library of Medicine Medical Subject Headings (MeSH)

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1. 喘息の治療において5-リポキシゲナーゼ経路に影響する薬剤 agents affecting the 5 lipoxygenase pathway in the treatment of asthma
2. 12歳未満の小児における慢性喘息：持続性喘息の治療およびコントロール薬 asthma in children younger than 12 years treatment of persistent asthma with controller medications
3. 成人における喘息の急性増悪の治療 treatment of acute exacerbations of asthma in adults
4. アレルギー性鼻炎の薬物療法 pharmacotherapy of allergic rhinitis
5. 喘息のマネージメントの概要 an overview of asthma management

English Journal

Efficacy of leukotriene receptor antagonist with anti-H1 receptor antagonist plus anti-H2 receptor antagonist for treatment of refractory chronic idiopathic urticaria.

Wan KS1, Chang YS.Author information 1Department of Pediatrics, Taipei City Hospital , Renai Branch , Taiwan and.AbstractBACKGROUND: The efficacy of the combination of leukotriene receptor antagonist (LRA) and H1 antihistamine was similar to the synergistic regimen of H1 and H2 antihistamine for treatment of chronic idiopathic urticaria (CIU). However, the effective rates of these two regimens were only 53.3% and 63.3%, respectively.
The Journal of dermatological treatment.J Dermatolog Treat.2014 Dec;25(6):459-61. doi: 10.3109/09546634.2013.849791. Epub 2013 Nov 5.
BACKGROUND: The efficacy of the combination of leukotriene receptor antagonist (LRA) and H1 antihistamine was similar to the synergistic regimen of H1 and H2 antihistamine for treatment of chronic idiopathic urticaria (CIU). However, the effective rates of these two regimens were only 53.3% and 63.3
PMID 24192062

Protective effect of pranlukast on Aβ 1-42-induced cognitive deficits associated with downregulation of cysteinyl leukotriene receptor 1.

Tang SS1, Ji MJ1, Chen L1, Hu M1, Long Y1, Li YQ1, Miao MX1, Li JC1, Li N2, Ji H1, Chen XJ2, Hong H1.Author information 1Department of Pharmacology, China Pharmaceutical University, Nanjing 210009, China.2Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, China.AbstractDeposition of extracellular amyloid-β (Aβ) peptide is one of the pathological hallmarks of Alzheimer's disease (AD). Accumulation of Aβ is thought to associate with cognition deficits, neuroinflammation and apoptosis observed in AD. However, effective neuroprotective approaches against Aβ neurotoxicity are unavailable. In the present study, we analysed the effects of pranlukast, a selective cysteinyl leukotriene receptor 1 (CysLT1R) antagonist, on the impairment of learning and memory formation induced by Aβ and the probable underlying electrophysiological and molecular mechanisms. We found that bilateral intrahippocampal injection of Aβ 1-42 resulted in a significant decline of spatial learning and memory of mice in the Morris water maze (MWM) and Y-maze tests, together with a serious depression of in vivo hippocampal long-term potentiation (LTP) in the CA1 region of the mice. Importantly, this treatment caused significant increases in CysLT1R expression and subsequent NF-κB signaling, caspase-3 activation and Bcl-2 downregulation in the hippocampus or prefrontal cortex. Oral administration of pranlukast at 0.4 or 0.8 mg/kg for 4 wk significantly reversed Aβ 1-42-induced impairments of cognitive function and hippocampal LTP in mice. Furthermore, pranlukast reversed Aβ 1-42-induced CysLT1R upregulation, and markedly suppressed the Aβ 1-42-triggered NF-κB pathway, caspase-3 activation and Bcl-2 downregulation in the hippocampus and prefrontal cortex in mice. Liquid chromatography-tandem mass spectrometry (LC-MS/MS) assay confirmed its presence in the brain after oral administration of pranlukast in mice. These data disclose novel findings about the therapeutic potential of pranlukast, revealing a previously unknown therapeutic possibility to treat memory deficits associated with AD.
The international journal of neuropsychopharmacology / official scientific journal of the Collegium Internationale Neuropsychopharmacologicum (CINP).Int J Neuropsychopharmacol.2014 Apr;17(4):581-92. doi: 10.1017/S1461145713001314. Epub 2013 Nov 11.
Deposition of extracellular amyloid-β (Aβ) peptide is one of the pathological hallmarks of Alzheimer's disease (AD). Accumulation of Aβ is thought to associate with cognition deficits, neuroinflammation and apoptosis observed in AD. However, effective neuroprotective approaches against Aβ neurot
PMID 24229499

Effectiveness of the leukotriene receptor antagonist pranlukast hydrate for the treatment of sleep disorder in patients with perennial allergic rhinitis.

Hara H1, Sugahara K, Hashimoto M, Mikuriya T, Tahara S, Yamashita H.Author information 1Department of Otolaryngology, Yamaguchi University Graduate School of Medicine , Ube, Yamaguchi , Japan.AbstractAbstract Conclusion: We found that addition of pranlukast to the conventional treatment for perennial allergic rhinitis may contribute to improvements in sleep disorder symptoms through a decrease in nasal congestion. Objective: We aimed to determine whether the leukotriene receptor antagonist pranlukast hydrate is effective in treating sleep disorder in patients with perennial allergic rhinitis. Methods: We conducted a questionnaire survey to determine the symptoms of rhinitis and sleep disturbances in 48 adult patients with perennial allergic rhinitis who visited the outpatient otolaryngology departments in hospitals in Yamaguchi Prefecture, Japan. The subjects presented with nasal symptoms and symptoms of sleep disorder during the last 2 weeks of treatment for allergic rhinitis that lasted for at least 1 month. A questionnaire based on the Pittsburgh Sleep Quality Index and Athens Insomnia Scale with some modifications was administered before and 4 weeks after the addition of pranlukast to the conventional treatment. Results: Addition of pranlukast improved the symptoms of perennial allergic rhinitis, with responses to all items of the questionnaire administered 4 weeks after pranlukast addition indicating significant improvements. Furthermore, the improvement in sleep disorder symptoms significantly correlated with improvement in nasal congestion, but not with improvements in sneezing and nasal discharge.
Acta oto-laryngologica.Acta Otolaryngol.2014 Mar;134(3):307-13. doi: 10.3109/00016489.2013.861926. Epub 2014 Jan 27.
Abstract Conclusion: We found that addition of pranlukast to the conventional treatment for perennial allergic rhinitis may contribute to improvements in sleep disorder symptoms through a decrease in nasal congestion. Objective: We aimed to determine whether the leukotriene receptor antagonist pranl
PMID 24460152

Japanese Journal

東京都における遷延性・慢性咳嗽および咳喘息の診療実態調査

切士紗織,原香織,久保綾子 [他]
アレルギー・免疫 21(12), 1942-1949, 2014-12
NAID 40020269765

Cysteinyl leukotriene receptor antagonist regulates allergic airway inflammation in an organ- and cytokine-specific manner

Kawano Tetsuya,Matsuse Hiroto,Tsuchida Tomoko,Fukahori Susumu,Fukushima Chizu,Nishino Tomoya,Kohno Shigeru
Medical Science Monitor 20, 297-302, 2014-02-22
… Cys-LT receptor antagonists (LTRAs) decrease allergic airway inflammation. …
NAID 120005438870

救急病院における喘息患者の治療実態アンケート : 兵庫県喘息死ゼロ作戦活動報告

堀朱矢,西村善博,新家治子,櫨木暢子,小林和幸,片山覚
アレルギー 63(1), 52-60, 2014-02-01
【目的】救急現場の喘息治療の実態を把握することを目的とした.【方法】2010年4月から1年間の救急診療状況について,兵庫県下の2次・3次救急を扱う175医療機関に対しアンケート調査を実施し, 2次医療圏ごとに検討した.【結果】143医療機関(回答率81.7%)から回答を得た.救急処置室での治療薬としては,ステロイド注射薬やアミノフィリン注射用製剤,SABAが多くの地区で選択されていた(順に平均86 …
NAID 110009798513

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リンク元	「ロイコトリエン受容体拮抗薬」「ロイコトリエン受容体遮断薬」「LTRA」「leukotriene antagonist」
拡張検索	「leukotriene receptor antagonists」
関連記事	「leukotriene receptor」「leukotriene」「leukotrienes」

「ロイコトリエン受容体拮抗薬」

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英: leukotriene receptor antagonist, LTRA
関: ロイコトリエン拮抗薬、ロイコトリエン受容体遮断薬、抗SRS-A剤

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ロイコトリエン受容体拮抗薬 LTRA : 約 23,900 件
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「ロイコトリエン受容体遮断薬」

　　[★]

英: leukotriene receptor antagonist
関: ロイコトリエン受容体拮抗薬

「LTRA」

　　[★] ロイコトリエン受容体拮抗薬 leukotriene receptor antagonist

「leukotriene antagonist」

　　[★]

ロイコトリエン拮抗薬

関: leukotriene receptor antagonist

「leukotriene receptor antagonists」

　　[★] ロイコトリエン受容体拮抗薬 LTRAs

「leukotriene receptor」

　　[★]

ロイコトリエン受容体、ロイコトリエンレセプター

「leukotriene」

　　[★] ロイコトリエン LT

「leukotrienes」