Tìm theo
Dimetindene
Các tên gọi khác (1) :
  • Dimethindene
Thuốc chống dị ứng
Thuốc Gốc
Small Molecule
CAS: 5636-83-9
ATC: D04AA13, R06AB03
CTHH: C20H24N2
PTK: 292.418
Dimetindene (Fenistil) is an antihistamine/anticholinergic used orally and locally as an antipruritic.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C20H24N2
Phân tử khối
292.418
Monoisotopic mass
292.193948778
InChI
InChI=1S/C20H24N2/c1-15(19-10-6-7-12-21-19)20-17(11-13-22(2)3)14-16-8-4-5-9-18(16)20/h4-10,12,15H,11,13-14H2,1-3H3
InChI Key
InChIKey=MVMQESMQSYOVGV-UHFFFAOYSA-N
IUPAC Name
dimethyl(2-{3-[1-(pyridin-2-yl)ethyl]-1H-inden-2-yl}ethyl)amine
Traditional IUPAC Name
dimethindene
SMILES
CC(C1=C(CCN(C)C)CC2=CC=CC=C12)C1=CC=CC=N1
Độ tan chảy
158
Độ hòa tan
239 mg/L (at 37 °C)
logP
3.74
logS
-3.9
pKa (strongest acidic)
18.93
pKa (Strongest Basic)
9.7
PSA
16.13 Å2
Refractivity
93.57 m3·mol-1
Polarizability
34.9 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Dimethindene occurs as a racemic mixture. The (S)-(+)-dimethindene is a potent M2-selective muscarinic receptor antagonist (with lower affinity for M1, M3, and M4 muscarinic receptors). The (R)-(-)-enantiomer is the eutomer (responsible for bioactivity) for histamine H1 receptor binding.
Cơ Chế Tác Dụng : Dimetindene (Fenistil) is an antihistamine/anticholinergic used orally and locally as an antipruritic. Dimethindene is a selective histamine H1 antagonist and binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
Độc Tính : As with other antihistaminic drugs, overdosage can produce the following symptoms: CNS depression accompanied by drowsiness (especially in adults), CNS stimulation and antimuscarinic effects (especially in children) including the following: excitation, ataxia, hallucinations, tonic or clonic spasms, mydriasis, dryness of the mouth, redness of the face, urine retention, fever and tachycardia. Blood hypotension is also possible. In its terminal phase, coma can be aggravated by cardiorespiratory colapse and death. There has been no report of a fatal outcome of Dimethindene overdosage.
Chỉ Định : Indicated as symptomatic treatment of allergic reactions: urticaria, allergies of the upper respiratory tract such as hey fever and perennial rhinitis, food and drug allergies; pruritus of various origins, except pruritus due to cholestasis; insect bites. Dimethindene is also indicated for pruritus in eruptive skin diseases such as chicken-pox. Dimethindene can also be used as an adjuvant in eczema and other pruriginous dermatoses of allergic origin.
Liều Lượng & Cách Dùng : Capsule - Oral - 4mg
Liquid - Topical - 0.1g/100mL
Syrup - Oral - 0.01g/100mL
Tablet, coated - Oral - 1mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Novartis
    Sản phẩm biệt dược : Fenistil
  • Công ty : Novartis
    Sản phẩm biệt dược : Foristal
  • Công ty : Novartis
    Sản phẩm biệt dược : Vibrocil
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08801
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D07853
ChemSpider
http://www.chemspider.com/Chemical-Structure.20541.html
PharmGKB
http://www.pharmgkb.org/drug/PA165958420
Wikipedia
http://en.wikipedia.org/wiki/Dimetindene
... loading
... loading