Tìm theo
Emedastine
Các tên gọi khác (7 ) :
  • 1-(2-Ethoxy-ethyl)-2-(4-methyl-[1,4]diazepan-1-yl)-1H-benzoimidazole
  • 1-(2-Ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)benzimidazole
  • 1-[2-(Ethoxy)ethyl]-2-(4-methyl-1-homopiperazinyl)benzimidazole
  • Emedastina
  • EMEDASTINE
  • Emedastine difumarate
  • Emedastinum
Thuốc chống dị ứng
Thuốc Gốc
Small Molecule
CAS: 87233-61-2
ATC: S01GX06
ĐG : Alcon Laboratories , http://www.alcon.com
CTHH: C17H26N4O
PTK: 302.4145
Emedastine is an antihistamine used in eye drops to treat allergic conjunctivitis. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H26N4O
Phân tử khối
302.4145
Monoisotopic mass
302.210661474
InChI
InChI=1S/C17H26N4O/c1-3-22-14-13-21-16-8-5-4-7-15(16)18-17(21)20-10-6-9-19(2)11-12-20/h4-5,7-8H,3,6,9-14H2,1-2H3
InChI Key
InChIKey=KBUZBQVCBVDWKX-UHFFFAOYSA-N
IUPAC Name
1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-1,3-benzodiazole
Traditional IUPAC Name
emedastine
SMILES
CCOCCN1C(=NC2=CC=CC=C12)N1CCCN(C)CC1
Độ hòa tan
Soluble (difumarate formulation)
logP
2.6
logS
-2.3
pKa (Strongest Basic)
8.68
PSA
33.53 Å2
Refractivity
90.47 m3·mol-1
Polarizability
35.49 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
4
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Emedastine is a relatively selective H1-receptor antagonist.
Cơ Chế Tác Dụng : Emedastine is an antihistamine used in eye drops to treat allergic conjunctivitis. [Wikipedia] Emedastine is a relatively selective, histamine H1 antagonist. In vitro examinations of emedastine's affinity for histamine receptors demonstrate relative selectivity for the H1 histamine receptor. In vivo studies have shown concentration-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva following topical ocular administration. Emedastine appears to be devoid of effects on adrenergic, dopaminergic and serotonin receptors.
Dược Động Học :
▧ Absorption :
Ophthalmic use of emedastine usually does not produce measurable plasma concentrations.
▧ Metabolism :
Two primary metabolites, 5-hydroxyemedastine and 6-hydroxyemedastine, are excreted in the urine as both free and conjugated forms. The 5'-oxoanalogs of 5-hydroxyemedastine and 6-hydroxy-emedastine and the N-oxide are also formed as minor metabolites.
▧ Route of Elimination :
Approximately 44% of the oral dose is recovered in the urine over 24 hours with only 3.6% of the dose excreted as parent drug. Two primary metabolites, 5- and 6-hydroxyemedastine, are excreted in the urine as both free and conjugated forms.
▧ Half Life :
The elimination half-life of oral emedastine in plasma is 3-4 hours.
Độc Tính : Somnolence and malaise have been reported following daily oral administration.
Chỉ Định : For the temporary relief of the signs and symptoms of allergic conjunctivitis.
Liều Lượng & Cách Dùng : Liquid - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Emadine
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01084
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3219
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505109
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07785
ChemSpider
http://www.chemspider.com/Chemical-Structure.3106.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50019624
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0065-0325-05
PharmGKB
http://www.pharmgkb.org/drug/PA164751802
Wikipedia
http://en.wikipedia.org/wiki/Emedastine
RxList
http://www.rxlist.com/cgi/generic2/emedastine.htm
Drugs.com
http://www.drugs.com/mtm/emedastine-ophthalmic.html
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