Tìm theo
Nepafenac
Các tên gọi khác (9 ) :
  • 2-amino-3-Benzoylbenzeneacetamide
  • AHR 9434
  • AHR-9434
  • AL 6515
  • AL-6515
  • Amfenac amide
  • Nepafenaco
  • Nepafenacum
  • Nevanac
anti inflammatory agents, anti inflammatory agents non steroidal, prodrugs
Thuốc Gốc
Small Molecule
CAS: 78281-72-8
ATC: S01BC10
CTHH: C15H14N2O2
PTK: 254.2839
Nepafenac is a non-steroidal anti-inflammatory prodrug (NSAID) usually sold as a prescription eye drop. It is used to treat pain and inflammation associated with cataract surgery.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H14N2O2
Phân tử khối
254.2839
Monoisotopic mass
254.105527702
InChI
InChI=1S/C15H14N2O2/c16-13(18)9-11-7-4-8-12(14(11)17)15(19)10-5-2-1-3-6-10/h1-8H,9,17H2,(H2,16,18)
InChI Key
InChIKey=QEFAQIPZVLVERP-UHFFFAOYSA-N
IUPAC Name
2-(2-amino-3-benzoylphenyl)acetamide
Traditional IUPAC Name
nepafenac
SMILES
NC(=O)CC1=CC=CC(C(=O)C2=CC=CC=C2)=C1N
Độ hòa tan
1.97e-02 g/l
logP
2.08
logS
-4.1
pKa (strongest acidic)
15.82
pKa (Strongest Basic)
1.83
PSA
86.18 Å2
Refractivity
74.46 m3·mol-1
Polarizability
26.63 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Low but quantifiable plasma concentrations of nepafenac and amfenac were observed in the majority of subjects 2 and 3 hours postdose, respectively, following bilateral topical ocular TID dosing of nepafenac ophthalmic suspension, 0.1%. The mean steady-state Cmax for nepafenac and for amfenac were 0.310 ± 0.104 ng/ml and 0.422 ± 0.121 ng/ml, respectively, following ocular administration.
Cơ Chế Tác Dụng : Nepafenac is a non-steroidal anti-inflammatory prodrug (NSAID) usually sold as a prescription eye drop. It is used to treat pain and inflammation associated with cataract surgery. Nepafenac is a prodrug. After penetrating the cornea, nepafenac undergoes rapid bioactivation to amfenac, which is a potent NSAID that uniformly inhibits the COX1 and COX2 activity.
Dược Động Học :
▧ Absorption :
Nepafenac rapidly cross the cornea (6 times faster than diclofenac in vitro).
▧ Protein binding :
Amfenac has high affinity toward serum albumin proteins. In vitro, the percent bound to human albumin and human serum was 95.4% and 99.1% respectively.
▧ Metabolism :
Nepafenac (prodrug) is deaminated to amfenac (active compound) in the ciliary body epithelium, retina, and choroid by intraocular hydrolases. Subsequently, amfenac undergoes extensive metabolism to more polar metabolites involving hydroxylation of the aromatic ring leading to glucuronide conjugate formation.
▧ Route of Elimination :
After oral administration of 14C-nepafenac to healthy volunteers, urinary excretion was found to be the major route of radioactivity elimination, accounting for approximately 85% of the dose, while fecal excretion represented approximately 6% of the dose. Nepafenac (prodrug) and amfenac (active compound) were not quantifiable in the urine.
Độc Tính : Ocularly applied non-steroidal anti-inflammatory drugs may cause increased bleeding of ocular tissues (including hyphemas) in conjunction with ocular surgery.
Chỉ Định : For the treatment of pain and inflammation associated with cataract surgery.
Tương Tác Thuốc :
Liều Lượng & Cách Dùng : Suspension - Ophthalmic - 0.1%
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : ILEVRO
  • Công ty : Alcon
    Sản phẩm biệt dược : Nevanac
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06802
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=151075
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=99443294
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D05143
ChemSpider
http://www.chemspider.com/Chemical-Structure.133160.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0065-0002-01
PharmGKB
http://www.pharmgkb.org/drug/PA165958407
Wikipedia
http://en.wikipedia.org/wiki/Nepafenac
RxList
http://www.rxlist.com/nevanac-drug.htm
Drugs.com
http://www.drugs.com/ppa/nepafenac.html
... loading
... loading