エピナスチン
- 関
- epinastine hydrochloride
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/12/04 02:18:37」(JST)
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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 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
- Enerisant
- 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
- Mianserin
- Thioperamide
- Toreforant
- 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
- Perturbation of tyraminergic/octopaminergic function inhibits oviposition in the cattle tick Rhipicephalus (Boophilus) microplus.
- Cossío-Bayúgar R, Miranda-Miranda E, Narváez Padilla V, Olvera-Valencia F, Reynaud E.SourceCentro Nacional de Investigación Disciplinaria en Parasitología Veterinaria, Instituto Nacional de Investigaciones Forestales Agrícolas y Pecuarias INIFAP, Carr. Fed. Cuernavaca-Cuautla No. 8534, Jiutepec, Morelos, CP 62550, Mexico.
- Journal of insect physiology.J Insect Physiol.2012 May;58(5):628-33. Epub 2012 Feb 17.
- The cattle tick Rhipicephalus microplus, is one of the most damaging livestock ectoparasites. Tropical tick infestation limits the introduction of high-yield bovine varieties because they do not have immunity to the diseases transmitted by these ectoparasites. This tick is usually controlled with ch
- PMID 22343017
- Pharmacological characterization of adenosine receptors on isolated human bronchi.
- Calzetta L, Spina D, Cazzola M, Page CP, Facciolo F, Rendina EA, Matera MG.SourceDepartment of Internal Medicine, University of Rome "Tor Vergata," Italy.
- American journal of respiratory cell and molecular biology.Am J Respir Cell Mol Biol.2011 Dec;45(6):1222-31. Epub 2011 Jun 23.
- Adenosine induces airways obstruction in subjects with asthma, but the receptor subtype responsible remains unknown. The objectives of this study were to determine the pharmacological profile of adenosine receptor subtypes mediating contraction and to investigate the mechanism in normal and passivel
- PMID 21700958
Japanese Journal
- スギ花粉アレルギー性結膜炎に及ぼすエピナスチン塩酸塩点眼液の影響
- A Case of IgG4-Related Dacryoadenitis that Regressed Without Systemic Steroid Administration
- Ohshima Koh-ichi,Sato Yasuharu,Yoshino Tadashi
- Journal of Clinical and Experimental Hematopathology 53(1), 53-56, 2013
- … In addition to the observation of lacrimal gland lesions, the administration of epinastine hydrochloride at a dosage of 20 mg/day and 0.01% betamethasone eye drops twice a day to both eyes was commenced in order to treat both allergic rhinitis and allergic conjunctivitis. … The hypotheses of spontaneous remission and/or the effect of epinastine hydrochloride administration can be proposed regarding the mechanism by which the lacrimal gland lesion decreased in size. …
- NAID 130003366787
- スギ花粉症に対してステロイド鼻噴霧薬と抗ヒスタミン薬併用投与の意義はあるか?
- 市村 恵一,菊池 恒,今吉 正一郎
- 耳鼻咽喉科臨床 105(11), 1107-116, 2012-11-01
- … Group 1 received only intranasal mometasone furoate (MF), and group 2 received intranasal MF and oral epinastine hydrochloride. …
- NAID 10031128277
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 ...
- Identification Name Epinastine Accession Number DB00751 (APRD00043) Type small molecule Groups approved Description Epinastine is used for the prevention of itching associated with allergic conjunctivitis. It has a multi ...
Related Pictures
★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。
[★]
- 関
- epinastine