Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
325.226645889
InChI
InChI=1S/C19H27N5/c1-16-6-2-3-7-17(16)23-14-12-22(13-15-23)11-9-19-21-20-18-8-4-5-10-24(18)19/h2-3,6-7H,4-5,8-15H2,1H3
InChI Key
InChIKey=RFWZESUMWJKKRN-UHFFFAOYSA-N
IUPAC Name
1-(2-methylphenyl)-4-(2-{5H,6H,7H,8H-[1,2,4]triazolo[4,3-a]pyridin-3-yl}ethyl)piperazine
Traditional IUPAC Name
dapiprazole
SMILES
CC1=CC=CC=C1N1CCN(CCC2=NN=C3CCCCN23)CC1
pKa (Strongest Basic)
7.67
Refractivity
100.22 m3·mol-1
Dược Lực Học :
Dapiprazole is an alpha-adrenergic blocking agent. It produces miosis by blocking the alpha-adrenergic receptors on the dilator muscle of the iris. Dapiprazole produces no significant action on ciliary muscle contraction and thus, there are no changes in the depth of the anterior chamber of the thickness of the lens. It does not alter the IOP either in normal eyes or in eyes with elevated IOP. The rate of pupillary constriction may be slightly slower in clients with brown irises than in clients with blue or green irises.
Cơ Chế Tác Dụng :
Dapiprazole (U.S. trade name Rev-Eyes) is an alpha blocker. It is used to reverse mydriasis after eye examination. [Wikipedia]
Dapiprazole acts through blocking the alpha1-adrenergic receptors in smooth muscle. It produces miosis through an effect on the dilator muscle of the iris and does not have any significant activity on ciliary muscle contraction and, therefore does not induce a significant change in the anterior chamber depth or the thickness of the lens.
Dược Động Học :
▧ Absorption :
Systemic absorption is negligible.
Độc Tính :
Oral LD50 is 1189-2100 mg/kg in mice, rats and rabbits.
Chỉ Định :
Used in the treatment of iatrogenically induced mydriasis produced by adrenergic (phenylephrine) or parasympatholytic (tropicamide) agents used in certain eye examinations.
Tương Tác Thuốc :
-
Tamsulosin
Concomitant use of alpha1-adrenergic antagonists, Tamsulosin and Dapiprazole, may result in additive antihypertensive effects. Combination therapy is not recommended.
Liều Lượng & Cách Dùng :
Solution / drops - Ophthalmic