Tìm theo
Ketotifen
Các tên gọi khác (6 ) :
  • Alaway
  • Ketotifen Fumarate
  • Ketotifene
  • Ketotifene fumarate
  • Ketotifeno
  • Ketotifenum
Thuốc chống dị ứng & dùng trong các trường hợp quá mẫn
Thuốc Gốc
Small Molecule
CAS: 34580-14-8
ATC: R06AX17, S01GX08
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: C19H19NOS
PTK: 309.425
A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H19NOS
Phân tử khối
309.425
Monoisotopic mass
309.118734925
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
InChI Key
InChIKey=ZCVMWBYGMWKGHF-UHFFFAOYSA-N
IUPAC Name
2-(1-methylpiperidin-4-ylidene)-6-thiatricyclo[8.4.0.0^{3,7}]tetradeca-1(10),3(7),4,11,13-pentaen-8-one
Traditional IUPAC Name
ketotifen
SMILES
CN1CCC(CC1)=C1C2=C(SC=C2)C(=O)CC2=CC=CC=C12
Độ tan chảy
152-153
Độ hòa tan
7.87e-03 g/l
logP
2.2
logS
-4.6
pKa (strongest acidic)
12.3
pKa (Strongest Basic)
7.15
PSA
20.31 Å2
Refractivity
101.73 m3·mol-1
Polarizability
34.61 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.43
Dược Lực Học : Ketotifen is a fast acting non-competitive histamine antagonist. It inhibits the release of mediators from mast cells. It is a non-bronchodilator antiasthmatic drug (when taken orally).
Cơ Chế Tác Dụng : A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis. [PubChem] Ketotifen is a relatively selective, non-competitive histamine antagonist (H1-receptor) and mast cell stabilizer. Ketotifen inhibits the release of mediators from mast cells involved in hypersensitivity reactions. Decreased chemotaxis and activation of eosinophils have also been demonstrated. Ketotifen also inhibits cAMP phosphodiesterase. Properties of ketotifen which may contribute to its antiallergic activity and its ability to affect the underlying pathology of asthma include inhibition of the development of airway hyper-reactivity associated with activation of platelets by PAF (Platelet Activating Factor), inhibition of PAF-induced accumulation of eosinophils and platelets in the airways, suppression of the priming of eosinophils by human recombinant cytokines and antagonism of bronchoconstriction due to leukotrienes. Ketotifen inhibits of the release of allergic mediators such as histamine, leukotrienes C4 and D4(SRS-A) and PAF.
Dược Động Học :
▧ Absorption :
Following oral administration absorption is at least 60%
▧ Protein binding :
75%
▧ Metabolism :
Primarily hepatic. The main metabolite found in both plasma and urine is the inactive ketotifen-N-glucuronide. Nor-ketotifen, the N-demethylated metabolite, and the 10-alpha-hydroxyl derivative are the only other metabolites detectable in human urine.
▧ Half Life :
21 hours (for elimination)
Độc Tính : Adverse reactions include headaches, conjunctival injection and rhinitis.
Chỉ Định : Indicated as an add-on or prophylactic oral medication in the chronic treatment of mild atopic asthmatic children. Also used as self-medication for the temporary relief of itching of the eye due to allergic conjunctivitis (ophthalmic).
Tương Tác Thuốc :
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Ketotifen, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
  • Trimethobenzamide Trimethobenzamide and Ketotifen, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Ketotifen, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
  • Trospium Trospium and Ketotifen, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Liquid - Ophthalmic
Solution - Ophthalmic
Syrup - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Patron
    Sản phẩm biệt dược : Totifen
  • Công ty : Novartis
    Sản phẩm biệt dược : Zaditen
  • Công ty : Alcon
    Sản phẩm biệt dược : Zaditor
  • Công ty : Novartis
    Sản phẩm biệt dược : Zasten
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00920
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3827
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508921
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01332
ChemSpider
http://www.chemspider.com/Chemical-Structure.3695.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50002087
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/50580-732-05
PharmGKB
http://www.pharmgkb.org/drug/PA450152
Wikipedia
http://en.wikipedia.org/wiki/Ketotifen
RxList
http://www.rxlist.com/cgi/generic/ketotifen.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/zad1598.shtml
Drugs.com
http://www.drugs.com/cdi/ketotifen-drops.html
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