ケトチフェン
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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/05/14 15:39:09」(JST)
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Ketotifen
|
| Systematic (IUPAC) name |
| 4-(1-Methylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one |
| Clinical data |
| Trade names |
Zaditor[1] |
| AHFS/Drugs.com |
Micromedex Detailed Consumer Information |
| MedlinePlus |
a604033 |
|
Pregnancy
category
|
- US: C (Risk not ruled out)
|
|
Legal status
|
- US: Oral - Prescription; Eye Drops - OTC
|
|
Routes of
administration
|
Oral, Eye Drops |
| Pharmacokinetic data |
| Bioavailability |
60% |
| Protein binding |
75% |
| Metabolism |
Hepatic |
| Half-life |
12 Hours |
| Identifiers |
|
CAS Registry Number
|
34580-14-8 Y |
|
ATC code
|
R06AX17 S01GX08 |
| PubChem |
CID 3827 |
| DrugBank |
DB00920 Y |
| ChemSpider |
3695 Y |
| UNII |
HBD503WORO Y |
| KEGG |
D01332 Y |
| ChEMBL |
CHEMBL534 Y |
| Chemical data |
| Formula |
C19H19NOS |
|
Molecular mass
|
309.426 g/mol |
SMILES
- O=C3c1sccc1C(\c2c(cccc2)C3)=C4/CCN(C)CC4
|
InChI
-
InChI=1S/C19H19NOS/c1-20-9-6-13(7-10-20)18-15-5-3-2-4-14(15)12-17(21)19-16(18)8-11-22-19/h2-5,8,11H,6-7,9-10,12H2,1H3 Y
Key:ZCVMWBYGMWKGHF-UHFFFAOYSA-N Y
|
| Y (what is this?) (verify) |
Ketotifen is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer. It is most commonly sold as a salt with fumaric acid, ketotifen fumarate, and is available in two forms. In its ophthalmic form, it is used to treat allergic conjunctivitis,[2] or the itchy red eyes caused by allergies. In its oral form, it is used to prevent asthma attacks.
Contents
- 1 Uses
- 2 Side effects
- 3 Brands
- 4 See also
- 5 References
- 6 External links
Uses
Ketotifen relieves and prevents eye itchiness and/or irritation associated with most seasonal allergies. It starts working within minutes after administering the drops. The drug has not been studied in children under three.[2] The mean elimination half life is 12 hours.[3] Besides its anti-histaminic activity, it is also a functional leukotriene antagonist and a phosphodiesterase inhibitor.
The drug may also help relieve the symptoms of irritable bowel syndrome.[4]
Side effects
|
|
This section does not cite any references or sources. Please help improve this section by adding citations to reliable sources. Unsourced material may be challenged and removed. (June 2014) |
Side effects include drowsiness, weight gain, dry mouth, irritability, and increased nosebleeds.
Brands
Ketotifen is marketed under many brand names worldwide.[5]
See also
References
- ^ http://www.webmd.com/drugs/2/drug-17484/zaditor-opht/details
- ^ a b Zaditor prescribing information Novartis
- ^ Grahnén A; Lönnebo A; Beck O; Eckernäs SA; Dahlström B; Lindström B (May 1992). "Pharmacokinetics of ketotifen after oral administration to healthy male subjects". Biopharm Drug Dispos 13 (4): 255–262. doi:10.1002/bdd.2510130404. PMID 1600111.
- ^ Klooker, TK; Braak, B; Koopman, KE; Welting, O; Wouters, MM; Van Der Heide, S; Schemann, M; Bischoff, SC et al. (2010). "The mast cell stabiliser ketotifen decreases visceral hypersensitivity and improves intestinal symptoms in patients with irritable bowel syndrome". Gut 59 (9): 1213–21. doi:10.1136/gut.2010.213108. PMID 20650926.
- ^ drugs.com International availability of ketofin Page accessed April 21, 2015
External links
- Zaditor web site
- Alaway web site
|
Antihistamines (R06)
|
|
| Aminoalkyl ethers |
- Bromazine (bromodiphenhydramine)
- Carbinoxamine
- Clemastine
- Chlorphenoxamine
- Diphenylpyraline
- Diphenhydramine
- Doxylamine
- Orphenadrine
- Phenyltoloxamine
|
|
| Substituted alkylamines |
- Brompheniramine
- Chlorphenamine
- Dexbrompheniramine (+pseudoephedrine)
- Dexchlorpheniramine (+betamethasone)
- Dimetindene
- Pheniramine
- Talastine
|
|
| Substituted ethylenediamines |
- Chloropyramine
- Histapyrrodine
- Mepyramine
- Methapyrilene
- Tripelennamine (pyribenzamine)
|
|
| Phenothiazine derivatives |
- Alimemazine
- Hydroxyethylpromethazine
- Isothipendyl
- Mequitazine
- Methdilazine
- Oxomemazine
- Promethazine
|
|
| Piperazine derivatives |
- Buclizine
- Cetirizine
- Chlorcyclizine
- Cinnarizine
- Cyclizine
- Hydroxyzine
- Levocetirizine
- Meclizine
- Oxatomide
|
|
| 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)
|
|
| For topical use |
- Bamipine
- Chloropyramine
- Chlorphenoxamine
- Clemastine
- Dimetindene
- Diphenhydramine
- Isothipendyl
- Mepyramine
- Promethazine
- Thenalidine
|
|
|
Index of the immune system
|
|
| Description |
- Physiology
- cells
- autoantigens
- autoantibodies
- complement
- surface antigens
- IG receptors
|
|
| Disease |
- Allergies
- Immunodeficiency
- Immunoproliferative immunoglobulin disorders
- Hypersensitivity and autoimmune disorders
- Neoplasms and cancer
|
|
| Treatment |
- Procedures
- Drugs
- antihistamines
- immunostimulants
- immunosuppressants
- monoclonal antibodies
|
|
|
|
Histaminergics
|
|
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
|
|
| 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
|
|
| 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
|
|
| H4 |
- Agonists: 4-Methylhistamine
- α-Methylhistamine
- Histamine
- VUF-8430
- Antagonists: JNJ-7777120
- JNJ-38518168
- Mianserin
- Thioperamide
- VUF-6002
|
|
|
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)
|
|
| TAAR1 active |
- Amphetamine
- Methamphetamine
- MDMA
- Phenethylamine
|
|
|
|
Enzyme
(inhibitors) |
| HDC |
- Catechin
- Meciadanol
- Naringenin
- Tritoqualine
|
|
| HNMT |
- Amodiaquine
- Diphenhydramine
- Harmaline
- Metoprine
- Quinacrine
- SKF-91,488
- Tacrine
|
|
| DAO |
|
|
|
| Others |
|
|
|
Index of the respiratory system
|
|
| Description |
- Anatomy
- Physiology
- Development
|
|
| Disease |
- Congenital
- Neoplasms and cancer
- Chest trauma
- Infection
- common cold
- pneumonia
- tuberculosis
- Other
- Symptoms and signs
|
|
| Treatment |
- Procedures
- Drugs
- nasal
- throat
- obstructive airway diseases
- cough and cold
- histaminergics
- pulmonary arterial hypertension
- other
- Surgery
|
|
|
UpToDate Contents
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English Journal
- Novel delivery approach for ketotifen fumarate: dissofilms formulation using 3(2) experimental design: in vitro/in vivo evaluation.
- Fahmy RH, Badr-Eldin SM.SourceDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University , Cairo , Egypt.
- Pharmaceutical development and technology.Pharm Dev Technol.2014 Aug;19(5):521-30. doi: 10.3109/10837450.2013.800108. Epub 2013 May 28.
- Abstract Orally dissolving films (dissofilms) have gained increasing popularity and attention due to their ease of administration and avoidance of first pass metabolism. Ketotifen fumarate (KF) bioavailability is reported to be only ∼50% due to hepatic first-pass metabolism. Aiming to surmount thi
- PMID 23713715
- Ketotifen in the management of chronic urticaria: resurrection of an old drug.
- Sokol KC, Amar NK, Starkey J, Grant JA.SourceDivision of Allergy and Immunology, University of Texas Medical Branch, Galveston, Texas. Electronic address: Kcsokol@utmb.edu.
- Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology.Ann Allergy Asthma Immunol.2013 Dec;111(6):433-6. doi: 10.1016/j.anai.2013.10.003. Epub 2013 Oct 25.
- PMID 24267353
- Mast cell stabilization alleviates acute lung injury after orthotopic autologous liver transplantation in rats by downregulating inflammation.
- Zhang A, Chi X, Luo G, Hei Z, Xia H, Luo C, Wang Y, Mao X, Xia Z.SourceDepartment of Anesthesiology, The Third Affiliated Hospital of Sun Yat-sen University, Guangzhou City, People's Republic of China.
- PloS one.PLoS One.2013 Oct 8;8(10):e75262. doi: 10.1371/journal.pone.0075262.
- BACKGROUND: Acute lung injury (ALI) is one of the most severe complications after orthotopic liver transplantation. Amplified inflammatory response after transplantation contributes to the process of ALI, but the mechanism underlying inflammation activation is not completely understood. We have demo
- PMID 24116032
Japanese Journal
- Probing AKR1C30 and AKR1C31 with Site-Directed Mutagenesis: Identifying the Roles of Residues 54 and 56 in the Binding of Substrates and Inhibitors
- Endo Satoshi,Arai Yuki,Matsunaga Toshiyuki [他],Ikari Akira,El-Kabbani Ossama,Hara Akira,Kitade Yukio
- Biological and Pharmaceutical Bulletin 37(11), 1848-1852, 2014
- … AKR1C30 reduces two drugs (ketotifen and naloxone) and 17-keto-5β-androstanes, whereas AKR1C31 does not reduce the two drugs, but is active towards loxoprofen and various 3/17/20-ketosteroids. …
- NAID 130004703904
- 経口メチルセルロース/アルギン酸液剤の物性に及ぼす薬物の影響
- 下山 哲哉,浦木 睦,高橋 彩,小林 正拓,高畑 雅臣,牧野 陽佑,伊藤 邦彦,小林 道也
- 薬剤学 74(1), 73-83, 2014
- … The present study aimed to determine how the addition of drugs (acetaminophen, mexiletine, metoprolol, ambroxol, loxoprofen, theophylline, ketotifen and salbutamol) affects the rheological and in vitro drug release characteristics of a 2% methylcellulose formulation and of a 2% methylcellulose/0.5% alginate formulation. …
- NAID 130003398001
- Mathematical Analysis on the Release of Ketotifen from Silicone Pressure-Sensitive Adhesive Matrices Containing Its Crystalline or Amorphous Form
- INOUE Kazuhiro,SUGIBAYASHI Kenji
- Journal of chemical engineering of Japan 45(8-12), 881-887, 2012-12
- NAID 40019532548
Related Links
- Ophthalmic ketotifen is used to relieve the itching of allergic pinkeye. Ketotifen is in a class of medications called antihistamines. It works by ... Ophthalmic ketotifen comes as a solution (liquid) to instill in the eye. It is ...
- Exposure to substances such as pollen, animal fur or house dust mite can cause your body to produce allergic symptoms treatable by Ketotifen ... Never take more than the prescribed dose. If you suspect that you or someone else ...
Related Pictures
★リンクテーブル★
[★]
- 英
- ketotifen
- 化
- フマル酸ケトチフェン ketotifen fumarate
- 商
- ザジテン、ジキリオン、エレクター、ケトテン、サジフェン、サラチン、サルジメン、スプデル、セキトン、デズワルト、ニチカード、フサコール、フマルトン、フマルフェン、ベナンザ、マゴチフェン
- 関
- 抗ヒスタミン薬
- 眼科用剤
- アレルギー性抗ヒスタミン薬
- H1受容体拮抗作用
- 肥満細胞からの化学伝達物質遊離抑制作用
薬物名
禁忌
- 本剤に対する過敏症
- てんかん、およびその既往(発作の閾値を下げるため)
[★]
ケトチフェン。フマル酸ケトチフェン