Tìm theo
Epinastine
Các tên gọi khác (6 ) :
  • (+-)-Epinastine
  • 3-amino-9,13b-dihydro-1H-Dibenz(c,F)imidazo(1,5-a)azepine
  • Epinastin
  • Epinastina
  • Epinastine
  • Epinastinum
histamine h1 antagonists, histamine antagonists, ophthalmics
Thuốc Gốc
Small Molecule
CAS: 80012-43-7
ATC: R06AX24, S01GX10
ĐG : Allergan Inc. , http://www.allergan.com
CTHH: C16H15N3
PTK: 249.3104
Epinastine is used for the prevention of itching associated with allergic conjunctivitis. It has a multi-action effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H15N3
Phân tử khối
249.3104
Monoisotopic mass
249.126597495
InChI
InChI=1S/C16H15N3/c17-16-18-10-15-13-7-3-1-5-11(13)9-12-6-2-4-8-14(12)19(15)16/h1-8,15H,9-10H2,(H2,17,18)
InChI Key
InChIKey=WHWZLSFABNNENI-UHFFFAOYSA-N
IUPAC Name
2,4-diazatetracyclo[12.4.0.0^{2,6}.0^{7,12}]octadeca-1(14),3,7(12),8,10,15,17-heptaen-3-amine
Traditional IUPAC Name
epinastine
SMILES
NC1=NCC2N1C1=CC=CC=C1CC1=CC=CC=C21
Độ tan chảy
205-208 °C
Độ hòa tan
1.63e-01 g/l
logP
3.51
logS
-3.2
pKa (Strongest Basic)
8.77
PSA
41.62 Å2
Refractivity
76.9 m3·mol-1
Polarizability
27.33 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Epinastine is an antihistamine and an inhibitor of histamine release from the mast cell for topical administration to the eyes. Epinastine is indicated for the prevention of itching associated with allergic conjunctivitis. Epinastine is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from the mast cell. Epinastine is selective for the histamine H1-receptor and has affinity for the histamine H2 receptor. Epinastine also possesses affinity for the a1-, a2-, and 5-HT2 -receptors. Epinastine does not penetrate the blood/brain barrier and, therefore, is not expected to induce side effects of the central nervous system.
Cơ Chế Tác Dụng : Epinastine is used for the prevention of itching associated with allergic conjunctivitis. It has a multi-action effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response. Epinastine has a multiaction effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response.
Dược Động Học :
▧ Absorption :
The absolute bioavailability of epinastine is about 40%.
▧ Protein binding :
64%
▧ Metabolism :
Mainly excreted unchanged, less than 10% metabolized.
▧ Route of Elimination :
Epinastine is mainly excreted unchanged. The renal elimination is mainly via active tubular secretion.
▧ Half Life :
12 hours
▧ Clearance :
* 56 L/hr [patients with allergic conjunctivitis receiving one drop of ELESTAT® ophthalmic solution in each eye twice daily for seven days]
Chỉ Định : For the prevention of itching associated with allergic conjunctivitis.
Liều Lượng & Cách Dùng : Solution / drops - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00751
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3241
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509056
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01713
ChemSpider
http://www.chemspider.com/Chemical-Structure.3128.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0023-9201-05
PharmGKB
http://www.pharmgkb.org/drug/PA164764489
Wikipedia
http://en.wikipedia.org/wiki/Epinastine
RxList
http://www.rxlist.com/cgi/generic3/elestat.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ele1680.shtml
Drugs.com
http://www.drugs.com/cdi/epinastine.html
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