ケトチフェン。フマル酸ケトチフェン
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/11/27 06:51:34」(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 |
Biological half-life |
12 Hours |
Identifiers |
CAS Number |
34580-14-8 Y |
ATC code |
R06AX17 S01GX08 |
PubChem |
CID: 3827 |
IUPHAR/BPS |
7206 |
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 (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
- 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
- Enerisant
- 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
- Mianserin
- Thioperamide
- Toreforant
- 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
- C-kit is important for SOD1(G93A) mouse survival independent of mast cells.
- Staats KA1, Schönefeldt S2, Van Helleputte L3, Van Rillaer M1, Lampi Y2, Dooley J2, Van Den Bosch L4, Liston A5.
- Neuroscience.Neuroscience.2015 Aug 20;301:415-20. doi: 10.1016/j.neuroscience.2015.06.026. Epub 2015 Jun 23.
- Amyotrophic Lateral Sclerosis (ALS) is a devastating neurodegenerative disease leading to progressive and lethal paralysis. The disease process is multi-factorial and is characterized by selective motor neuron degeneration. Previous work demonstrated that the local concentration of various growth fa
- PMID 26112382
- Differences in Features and Course of Mucosal Type Eosinophilic Gastroenteritis between Korean Infants and Children.
- Choi BS1, Hong SJ2, Park SH1, Kim HM1, Choe BH1.
- Journal of Korean medical science.J Korean Med Sci.2015 Aug;30(8):1129-35. doi: 10.3346/jkms.2015.30.8.1129. Epub 2015 Jul 15.
- Eosinophilic gastroenteritis (EGE) is a disorder characterized by eosinophilic infiltration of the bowel wall and various gastrointestinal (GI) manifestations. This study aimed to evaluate the characteristics of EGE in infants and children. A total of 22 patients were diagnosed with histologic EGE (
- PMID 26240491
- Mast cell degranulation inhibits motor patterns of human ileum and sigmoid colon in vitro: relevance for postoperative ileus.
- Rychter J1,2, Ortega O3, Berdun S2, Arenas C1, Lopez I3, Espin F3, Vergara P1,2, Clavé P1,3.
- Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society.Neurogastroenterol Motil.2015 Aug;27(8):1098-109. doi: 10.1111/nmo.12589. Epub 2015 May 13.
- BACKGROUND: Local release of mast cell proteases during gastrointestinal surgery is associated with the inhibition of motility and postoperative ileus (POI). We determined whether activation of intramuscular mast cell affects the motor patterns of the human ileum and colon and whether proteases are
- PMID 25974622
Japanese Journal
- 健康成人における抗ヒスタミン薬の中枢抑制作用に関する研究:―オロパタジン・フマル酸ケトチフェン・フェキソフェナジンの比較―
- オロパタジン塩酸塩の小児アトピー性皮膚炎に対する二重盲検比較試験
- Okicamelliaside, an Extraordinarily Potent Anti-Degranulation Glucoside Isolated from Leaves of Camellia japonica
- Bioscience, biotechnology, and biochemistry 74(12), 2532-2534, 2010-12-23
- NAID 10027728538
Related Links
- Ketotifen Fumarate Drug Information from Drugs.com. Includes Ketotifen Fumarate side effects, interactions and indications.
- Learn about the prescription medication Zaditor (Ketotifen Fumarate), drug uses, dosage, side effects, drug interactions, warnings, reviews and patient labeling.
★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)
[★]
フマル酸、フマル酸塩、フマル酸エステル
- 関
- fumaric acid