- 関
- epinastine
WordNet
- a complex consisting of an organic base in association with hydrogen chloride
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/08/13 10:47:01」(JST)
[Wiki en表示]
Epinastine
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Systematic (IUPAC) name |
(RS)-3-amino-9,13b-dihydro-1H-dibenz(c,f)imidazo(1,5-a)azepine
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Clinical data |
Trade names |
Alesion, Elestat, Purivist, Relestat |
AHFS/Drugs.com |
monograph |
MedlinePlus |
a604011 |
Pregnancy
category |
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Routes of
administration |
Eye drops |
Pharmacokinetic data |
Protein binding |
64% |
Biological half-life |
12 hours |
Identifiers |
CAS Registry Number |
80012-43-7 Y |
ATC code |
R06AX24 S01GX10 |
PubChem |
CID: 3241 |
IUPHAR/BPS |
7176 |
DrugBank |
DB00751 Y |
ChemSpider |
3128 Y |
UNII |
Q13WX941EF Y |
KEGG |
D07900 Y |
ChEBI |
CHEBI:51032 Y |
ChEMBL |
CHEMBL1106 Y |
Chemical data |
Formula |
C16H15N3 |
Molecular mass |
249.311 g/mol |
SMILES
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N\4=C(\N3c1c(cccc1)Cc2c(cccc2)C3C/4)N
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InChI
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InChI=1S/C16H15N3/c17-16-18-10-15-13-7-3-1-5-11(13)9-12-6-2-4-8-14(12)19(15)16/h1-8,15H,9-10H2,(H2,17,18) Y
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Key:WHWZLSFABNNENI-UHFFFAOYSA-N Y
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Y (what is this?) (verify) |
Epinastine (brand names Alesion, Elestat, Purivist, Relestat) is a second-generation antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis. It is produced by Allergan and marketed by Inspire in the United States.[1] It is highly selective for the H1 receptor and does not cross the blood-brain-barrier.[2]
References
- ^ Pradhan, S; Abhishek, K; Mah, F (2009). "Epinastine: topical ophthalmic second generation antihistamine without significant systemic side effects". Expert opinion on drug metabolism & toxicology 5 (9): 1135–40. doi:10.1517/17425250903117284. PMID 19630694.
- ^ Walther G, Daniel H, Bechtel WD, Brandt K (April 1990). "New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine". Arzneimittel-Forschung 40 (4): 440–6. PMID 1972625.
External links
- Official U.S. website of Elestat
Antihistamines (R06)
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Aminoalkyl ethers |
- Bromazine (bromodiphenhydramine)
- Carbinoxamine
- Clemastine
- Chlorphenoxamine
- Diphenylpyraline
- Diphenhydramine
- Doxylamine
- Orphenadrine
- Phenyltoloxamine
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Substituted alkylamines |
- Brompheniramine
- Chlorphenamine
- Dexbrompheniramine (+pseudoephedrine)
- Dexchlorpheniramine (+betamethasone)
- Dimetindene
- Pheniramine
- Talastine
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Substituted ethylenediamines |
- Chloropyramine
- Histapyrrodine
- Mepyramine
- Methapyrilene
- Tripelennamine (pyribenzamine)
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Phenothiazine derivatives |
- Alimemazine
- Hydroxyethylpromethazine
- Isothipendyl
- Mequitazine
- Methdilazine
- Oxomemazine
- Promethazine
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Piperazine derivatives |
- Buclizine
- Cetirizine
- Chlorcyclizine
- Cinnarizine
- Cyclizine
- Hydroxyzine
- Meclizine
- Oxatomide
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Others for systemic use |
- Antazoline
- Azatadine
- Bamipine
- Cyproheptadine
- Deptropine
- Ebastine
- Emedastine
- Epinastine
- Ketotifen
- Latrepirdine
- Mebhydrolin
- Mizolastine
- Olopatadine
- Phenindamine
- Pimethixene
- Pyrrobutamine
- Quifenadine
- Rupatadine
- Triprolidine
- selective (Acrivastine
- Astemizole
- Azelastine
- Bilastine
- Desloratadine
- Fexofenadine
- Loratadine
- Terfenadine)
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For topical use |
- Bamipine
- Chloropyramine
- Chlorphenoxamine
- Clemastine
- Dimetindene
- Diphenhydramine
- Isothipendyl
- Mepyramine
- Promethazine
- Thenalidine
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Index of the immune system
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Description |
- Physiology
- cells
- autoantigens
- autoantibodies
- complement
- surface antigens
- IG receptors
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Disease |
- Allergies
- Immunodeficiency
- Immunoproliferative immunoglobulin disorders
- Hypersensitivity and autoimmune disorders
- Neoplasms and cancer
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Treatment |
- Procedures
- Drugs
- antihistamines
- immunostimulants
- immunosuppressants
- monoclonal antibodies
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Histaminergics
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Receptor
(ligands) |
H1 |
- Agonists: 2-Pyridylethylamine
- Betahistine
- Histamine
- HTMT
- UR-AK49
- Antagonists: First-generation: 4-Methyldiphenhydramine
- Alimemazine
- Antazoline
- Azatadine
- Bamipine
- Benzatropine (benztropine)
- Bepotastine
- Bromazine
- Brompheniramine
- Buclizine
- Captodiame
- Carbinoxamine
- Chlorcyclizine
- Chloropyramine
- Chlorothen
- Chlorphenamine
- Chlorphenoxamine
- Cinnarizine
- Clemastine
- Clobenzepam
- Clocinizine
- Cyclizine
- Cyproheptadine
- Dacemazine
- Decloxizine
- Deptropine
- Dexbrompheniramine
- Dexchlorpheniramine
- Dimenhydrinate
- Dimetindene
- Diphenhydramine
- Diphenylpyraline
- Doxylamine
- Embramine
- Etodroxizine
- Etybenzatropine (ethylbenztropine)
- Etymemazine
- Flunarizine
- Histapyrrodine
- Homochlorcyclizine
- Hydroxyethylpromethazine
- Hydroxyzine
- Isopromethazine
- Isothipendyl
- Meclozine
- Medrylamine
- Mepyramine (pyrilamine)
- Mequitazine
- Methafurylene
- Methapyrilene
- Methdilazine
- Moxastine
- Orphenadrine
- Oxatomide
- Oxomemazine
- Phenindamine
- Pheniramine
- Phenyltoloxamine
- Pimethixene
- Piperoxan
- Pipoxizine
- Promethazine
- Propiomazine
- Pyrrobutamine
- Talastine
- Thenalidine
- Thenyldiamine
- Thiazinamium
- Thonzylamine
- Tolpropamine
- Tripelennamine
- Triprolidine
- Second/third-generation: Acrivastine
- Alinastine
- Astemizole
- Azelastine
- Bamirastine
- Barmastine
- Bepiastine
- Bepotastine
- Bilastine
- Cabastinen
- Carebastine
- Cetirizine
- Clemastine
- Clemizole
- Clobenztropine
- Desloratadine
- Dorastine
- Ebastine
- Efletirizine
- Emedastine
- Epinastine
- Fexofenadine
- Flezelastine
- Ketotifen
- Latrepirdine
- Levocabastine
- Levocetirizine
- Linetastine
- Loratadine
- Mapinastine
- Mebhydrolin
- Mizolastine
- Moxastine
- Noberastine
- Octastine
- Olopatadine
- Perastine
- Pibaxizine
- Piclopastine
- Rocastine
- Rupatadine
- Setastine
- Talastine
- Temelastine
- Terfenadine
- Vapitadine
- Zepastine
- Non-generational: Atypical antipsychotics (e.g., aripiprazole, asenapine, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, ziprasidone, zotepine)
- Tetracyclic antidepressants (e.g., amoxapine, loxapine, maprotiline, mianserin, mirtazapine, oxaprotiline)
- Tricyclic antidepressants (e.g., amitriptyline, butriptyline, clomipramine, desipramine, dosulepin (dothiepin), doxepin, imipramine, iprindole, lofepramine, nortriptyline, protriptyline, trimipramine)
- Typical antipsychotics (e.g., chlorpromazine, flupenthixol, fluphenazine, loxapine, perphenazine, prochlorperazine, thioridazine, thiothixene)
- Unknown/unsorted: Belarizine
- Elbanizine
- Flotrenizine
- Napactadine
- Tagorizine
- Trelnarizine
- Trenizine
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H2 |
- Agonists: Amthamine
- Betazole
- Dimaprit
- Histamine
- HTMT
- Impromidine
- UR-AK49
- Antagonists: Bisfentidine
- Burimamide
- Cimetidine
- Dalcotidine
- Donetidine
- Ebrotidine
- Etintidine
- Famotidine
- Lafutidine
- Lamtidine
- Lavoltidine (loxtidine)
- Lupitidine
- Metiamide
- Mifentidine
- Niperotidine
- Nizatidine
- Osutidine
- Oxmetidine
- Pibutidine
- Quisultazine (quisultidine)
- Ramixotidine
- Ranitidine
- Roxatidine
- Sufotidine
- Tiotidine
- Tuvatidine
- Venritidine
- Xaltidine
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H3 |
- Agonists: α-Methylhistamine
- Cipralisant
- Histamine
- Imetit
- Immepip
- Immethridine
- Methimepip
- Proxyfan
- Antagonists: A-349,821
- A-423,579
- ABT-239
- ABT-652
- AZD5213
- Betahistine
- Burimamide
- Ciproxifan
- Clobenpropit
- Conessine
- GSK-189,254
- Impentamine
- Iodophenpropit
- Irdabisant
- JNJ-5207852
- MK-0249
- NNC 38-1049
- PF-03654746
- Pitolisant
- SCH-79687
- Thioperamide
- VUF-5681
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H4 |
- Agonists: 4-Methylhistamine
- α-Methylhistamine
- Histamine
- VUF-8430
- Antagonists: JNJ-7777120
- JNJ-38518168
- Mianserin
- Thioperamide
- VUF-6002
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Transporter
(inhibitors) |
VMATs |
TAAR1 inactive |
- Amiodarone
- APP
- AZIK
- Bietaserpine
- Deserpidine
- Dihydrotetrabenazine
- Efavirenz
- GBR-12935
- GZ-793A
- Ibogaine
- Ketanserin
- Lobeline
- Methoxytetrabenazine
- NBI-98854
- Reserpine
- Rose bengal
- SD-809
- Tetrabenazine
- Vanoxerine (GBR-12909)
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TAAR1 active |
- Amphetamine
- Methamphetamine
- MDMA
- Phenethylamine
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Enzyme
(inhibitors) |
HDC |
- Catechin
- Meciadanol
- Naringenin
- Tritoqualine
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HNMT |
- Amodiaquine
- Diphenhydramine
- Harmaline
- Metoprine
- Quinacrine
- SKF-91,488
- Tacrine
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DAO |
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Others |
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Index of the respiratory system
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Description |
- Anatomy
- Physiology
- Development
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Disease |
- Congenital
- Neoplasms and cancer
- Chest trauma
- Infection
- common cold
- pneumonia
- tuberculosis
- Other
- Symptoms and signs
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Treatment |
- Procedures
- Drugs
- nasal
- throat
- obstructive airway diseases
- cough and cold
- histaminergics
- pulmonary arterial hypertension
- other
- Surgery
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UpToDate Contents
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English Journal
- Pharmacological Characterization of Adenosine Receptors on Isolated Human Bronchi.
- Calzetta L, Spina D, Cazzola M, Page CP, Facciolo F, Rendina EA, Matera MG.SourceInternal Medicine, University of Rome "Tor Vergata", Rome, Italy; The Sackler Institute of Pulmonary Pharmacology, Institute of Pharmaceutical Science, King's College London, London, United Kingdom.
- American journal of respiratory cell and molecular biology.Am J Respir Cell Mol Biol.2011 Jun 23. [Epub ahead of print]
- Rationale: Adenosine induces airways obstruction in asthmatic subjects but the receptor subtype responsible remains unknown. Objectives: To determine the pharmacological profile of adenosine receptor subtypes mediating contraction and to investigate the mechanism in normal and passively sensitized h
- PMID 21700958
- Octopamine and occupancy: an aminergic mechanism for intruder-resident aggression in crickets.
- Rillich J, Schildberger K, Stevenson PA.SourceInstitut fur Neurobiologie, Freie Universitat Berlin, Konigin-Luise-Str. 28-30, D-14195 Berlin, Germany.
- Proceedings. Biological sciences / The Royal Society.Proc Biol Sci.2011 Jun 22;278(1713):1873-80. Epub 2010 Nov 24.
- Aggression is a behavioural strategy for securing resources (food, mates and territory) and its expression is strongly influenced by their presence and value. While it is known that resource holders are generally highly aggressive towards intruding consexuals and usually defeat them, the underlying
- PMID 21106592
Japanese Journal
- アンギオテンシンII受容体拮抗薬が誘因と推察された舌・口底部の血管性浮腫の1例
- 坂元 亮一,上川 善昭,永山 知宏,杉原 一正
- 歯科薬物療法 29(1), 21-24, 2010-04-01
- … She visited an emergency hospital, and was prescribed serrapeptase, a complex of betamethasone and chlorpheniramine maleate, and epinastine hydrochloride. …
- NAID 10026132690
- 薬剤の臨床 小児アトピー性皮膚炎に対するエピナスチン塩酸塩ドライシロップの有用性
Related Links
- エピナスチン塩酸塩(Epinastine hydrochloride)の検索ならお薬検索QLife(キューライフ)。お医者さんが処方する処方薬と、薬局で買える市販薬(OTC)、の効果と副作用、写真、添付文書、保管方法等を掲載。商品名だけでなく一般名や剤 ...
- Epinastine Hydrochloride reference guide for safe and effective use from the American Society of Health-System Pharmacists (AHFS DI). ... References 1. Allergan. Elestat (epinastine hydrochloride) ophthalmic solution 0.05% ...
★リンクテーブル★
[★]
- 英
- epinastine
- 化
- エピナスチン塩酸塩、塩酸エピナスチン、epinastine hydrochloride
- 商
- アズサレオン、アスモット、アルピード、アレゲイン、アレジオテック、アレジオン、アレナピオン、アレルオフ、エピナジオン、エルピナン、チムケント、ピナジオン、ヘルボッツ、ユピテル
- 関
- その他のアレルギー用薬。抗ヒスタミン薬
- 「重要な基本的注意」として「眠気を催すことがあるので、本剤投与中の患者には自動車の運転等危険を伴う機械の操作に注意させること。」との記載有り。
[★]
エピナスチン
- 関
- epinastine hydrochloride
[★]
塩酸塩、ハイドロクロライド