Tìm theo
Difluprednate
Các tên gọi khác (3) :
  • DFBA
  • Difluoroprednisolone butyrate acetate
  • Durezol
anti inflammatory agents, glucocorticoids, corticosteroids
Thuốc Gốc
Small Molecule
CAS: 23674-86-4
ATC: D07AC19
CTHH: C27H34F2O7
PTK: 508.5515
Difluprednate is a topical corticosteroid indicated for the treatment of infammation and pain associated with ocular surgery. It is a butyrate ester of 6(α), 9(α)-difluoro prednisolone acetate. Difluprednate is abbreviated DFBA, or difluoroprednisolone butyrate acetate. It is indicated for treatment of endogenous anterior uveiti.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
508.5515
Monoisotopic mass
508.227259852
InChI
InChI=1S/C27H34F2O7/c1-5-6-23(34)36-26(22(33)14-35-15(2)30)10-8-17-18-12-20(28)19-11-16(31)7-9-24(19,3)27(18,29)21(32)13-25(17,26)4/h7,9,11,17-18,20-21,32H,5-6,8,10,12-14H2,1-4H3/t17-,18-,20-,21-,24-,25-,26-,27-/m0/s1
InChI Key
InChIKey=WYQPLTPSGFELIB-JTQPXKBDSA-N
IUPAC Name
(1R,2S,8S,10S,11S,14R,15S,17S)-14-[2-(acetyloxy)acetyl]-1,8-difluoro-17-hydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-14-yl butanoate
Traditional IUPAC Name
(1R,2S,8S,10S,11S,14R,15S,17S)-14-[2-(acetyloxy)acetyl]-1,8-difluoro-17-hydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-14-yl butanoate
SMILES
Độ tan chảy
191-194
Độ hòa tan
9.70e-03 g/l
logP
3
logS
-4.7
pKa (strongest acidic)
13.55
pKa (Strongest Basic)
-3.4
PSA
106.97 Å2
Refractivity
125.38 m3·mol-1
Polarizability
51.46 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Difluprednate is a corticosteroid used as an anti-inflammatory steroidal drug used primarily in ocular surgery.
Cơ Chế Tác Dụng : Difluprednate is a topical corticosteroid indicated for the treatment of infammation and pain associated with ocular surgery. It is a butyrate ester of 6(α), 9(α)-difluoro prednisolone acetate. Difluprednate is abbreviated DFBA, or difluoroprednisolone butyrate acetate. It is indicated for treatment of endogenous anterior uveiti. Corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins (lipocortins). It is postulated that these proteins control the biosynthesis of potent mediators of infammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
Dược Động Học :
▧ Absorption :
Difluprednate penetrates the corneal epithelium rapidly and effectively. Low systemic absorption.
▧ Metabolism :
Difluprednate is rapidly deacetylated in the aqueous humor to difluoroprednisolone butyrate (DFB), the drug’s active metabolite. Endogenous tissue esterases then metabolize DFB to the inert metabolite hydroxyfluoroprednisolone butyrate (HFB), which limits systemic exposure to the active compound.
▧ Route of Elimination :
78.5% of radioactivity was excreted aftert 24 hours, and 99.5% by 7 days after a single dose of labeled difluprednate instilled in the right eyes of pigmented rabbits.
Độc Tính : Preclinical pharmacokinetic and toxicity studies have established that difluprednate ophthalmic emulsion 0.05% given 4 times a day is not toxic to the eye.
Chỉ Định : For the treatment of inflammation and pain associated with ocular surgery.
Tương Tác Thuốc :
Liều Lượng & Cách Dùng : Emulsion - Ophthalmic - 0.05%
Emulsion - Ophthalmic - Instill 1 gtt in affected eye(s) QID x2 weeks, then BID x1 week, then taper and discontinue
Dữ Kiện Thương Mại
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