Ophthalmic drugs (cataract)
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Nepafenac

Ophthalmic drugs (cataract)
Product Name
Nepafenac
CAS No.
78281-72-8
Chemical Name
Nepafenac
Synonyms
Nevanac;AL 6515;AHR 9434;Nepafanac;Nepafenac;Nepafenac - WS;nepafenac,Nevance;2-Amino-3-benzoylbenzeneacetamide;2-(2-amino-3-benzoyl-phenyl)acetamide;(R)-(but-3-yn-2-yloxy)trimethylsilane
CBNumber
CB01116872
Molecular Formula
C15H14N2O2
Formula Weight
254.28
MOL File
78281-72-8.mol
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Nepafenac Property

Melting point:
177-181°C
storage temp. 
Refrigerator
solubility 
DMSO: ≥5mg/mL
form 
powder
color 
faint yellow to dark yellow
Merck 
14,6469
InChIKey
QEFAQIPZVLVERP-UHFFFAOYSA-N
CAS DataBase Reference
78281-72-8(CAS DataBase Reference)
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Safety

Hazard Codes 
N
Risk Statements 
50/53
Safety Statements 
60-61
RIDADR 
UN 3077 9 / PGIII
WGK Germany 
3
RTECS 
CY1480710
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H400Very toxic to aquatic life

Precautionary statements

P273Avoid release to the environment.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0288
Product name
Nepafenac
Purity
≥98% (HPLC)
Packaging
10mg
Price
$63.3
Updated
2018/11/13
Sigma-Aldrich
Product number
SML0288
Product name
Nepafenac
Purity
≥98% (HPLC)
Packaging
50mg
Price
$245
Updated
2018/11/13
TCI Chemical
Product number
N0932
Product name
Nepafenac
Purity
>98.0%(HPLC)(T)
Packaging
200mg
Price
$131
Updated
2018/11/22
TCI Chemical
Product number
N0932
Product name
Nepafenac
Purity
>98.0%(HPLC)(T)
Packaging
1g
Price
$458
Updated
2018/11/22
Cayman Chemical
Product number
23700
Product name
Nepafenac
Purity
≥98%
Packaging
10mg
Price
$35
Updated
2018/11/19
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Nepafenac Chemical Properties,Usage,Production

Ophthalmic drugs (cataract)

Nepafenac is a novel ophthalmic non-steroidal anti-inflammatory drug (NSAID), for the treatment of eye pain and inflammation caused by cataract surgery, compared with traditional NSAIDs, chemical structure of Nepafenac is conducive to make it rapidly penetrate the cornea and distribute to its target site, which is helpful to reduce the accumulation of the drug in the corneal surface and to reduce the incidence of complications of the eye surface, it has many advantages such as infiltration, targeting strong, little toxic side effects and so on.
August 19, 2005 ,the US Food and Drug Administration (FDA) approved nepafenac ophthalmic suspension for the treatment of cataract surgery-related pain and inflammation, it is the first ophthalmic NSAID prodrug formulation approved for marketing.
Nepafenac after ocular administration, can rapidly pass through the cornea , and under the action of eye tissue hydrolytic enzymes,it can become into ammonia diclofenac (a kind of NSAID); and ammonia diclofenac by inhibiting prostaglandin H synthase ( cyclooxygenase), can block prostaglandin synthesis to play its role as an anti-inflammatory analgesic. As is known, prostaglandin is one of the media causing ocular inflammation it can lead to blood-aqueous barrier crash, vasodilatation, increased vascular permeability and leukocyte chemotaxis, etc. In addition, prostaglandins can also control contraction of the iris sphincter through non-cholinergic mechanism which can trigger the miosis reaction during eye surgery and after surgery. After ocular administration of NSAIDs, it can inhibit prostaglandins synthesis in the iris, ciliary body and conjunctiva, so people can prevent eye inflammation, and reduce the associated pain.
The above information is edited by the chemicalbook of Tian Ye.

Description

Nepafenac, launched by Alcon Laboratories, is a topical ophthalmic medication indicated for the treatment of ocular pain and inflammation associated with cataract surgery. Nepafenac is a prodrug of amfenac, which is an NSAID and a potent non-selective inhibitor of COX-1 (IC50=0.25 μM)) and COX-2 (IC50=0.15μM). Nepefenac itself exhibits only weak activity against COX-1 (IC50=64.3μM). Amfenac (Fenazox) has been marketed in Japan since 1986 for the treatment of rheumatoid arthritis, post-surgical pain, and inflammation. With most NSAIDs that are currently being used as topical ophthalmic agents, the maximum drug concentration is achieved on the ocular surface, with progressively lower concentrations in the cornea, aqueous humor, vitreous, and retina. Nepafenac has been found to have a penetration coefficient that is 4 – 28 times greater than that achieved with conventional NSAIDs such as diclofenac, bromofenac, and ketorolac. In addition, the bioconversion of nepefenac to amfenac is primarily mediated by ocular tissue hydrolases, specifically in the iris, ciliary body, retina, and choroid. The enhanced permeability of nepefenac combined with rapid bioactivation in the ocular tissue translates into superior anti-inflammatory efficacy at the target sites. In preclinical models, a single topical ocular dose of nepefenac (0.1%) inhibits prostaglandin synthesis in the iris/ciliary body by 85–95% for more than 6 h, and in the retina/choroid by 55% for up to at least 4 h. By comparison, diclofenac (0.1%) shows 100% inhibition of prostaglandin synthesis in the iris/ciliary body for only 20 min, with 75% recovery observed within 6 h. Diclofenac’s inhibition of prostaglandin synthesis in the retina/choroids is minimal. The recommended dose of nepafenac ophthalmic suspension is one drop in the affected eye(s) three times daily beginning one day prior to cataract surgery, continued on the day of surgery and through the first two weeks of the postoperative period. Although the drug is applied topically, low but quantifiable plasma concentrations of nepefenac and amfenac are observed in majority of the subjects following t.i.d. dosing of nepefenac ophthalmic solution. The clinical significance of the systemic absorption of nepefenac after ophthalmic administration is unknown. The efficacy of nepafenac was demonstrated in two placebo-controlled clinical studies involving over 680 patients. Nepafenac suspension was dosed three times daily, beginning one day prior to cataract surgery, continuing on the day of surgery, and for 14 days postoperatively.

Chemical Properties

Light Yellow Solid

Originator

AH Robins (US)

Uses

Labelled Nepafenac (N390080). A non-steroidal anti-inflammatory with analgesic activity; selective COX-2 inhibitor. Prodrug of Amfenac.

Uses

Nepafenac is a non-steroidal anti-inflammatory drug (NSAID), usually sold as a prescription eye drop. It reduces pain and inflammation in the eyes. Nepafenac ophthalmic is used to reduce pain and swelling after cataract surgery. Its side effects may inclu

Definition

ChEBI: A monocarboxylic acid amide that is amfenac in which the carboxylic acid group has been converted to the corresponding carboxamide. It is a prodrug for amfenac, used in eye drops to treat pain and inflammation following cataract surgery.

brand name

Nevanac (Alcon).

Veterinary Drugs and Treatments

Nepafenac is a nonsteroidal anti-inflammatory and analgesic prodrug. After topical ocular dosing, nepafenac penetrates the cornea and is converted by ocular tissue hydrolases to amfenac, a nonsteroidal anti-inflammatory drug. Amfenac is thought to inhibit the action of prostaglandin H synthase (cyclooxygenase), an enzyme required for prostaglandin production. Nepafenac is indicated for the treatment of pain and inflammation associated with cataract surgery.

Nepafenac Preparation Products And Raw materials

Raw materials

Preparation Products

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Nepafenac Suppliers

Shanghai Orgpharma Chemical Co., Ltd.
Tel
+86 (21) 22062033
Email
info@orgpharma.cn
Country
China
ProdList
225
Advantage
55
Jinan Aery Pharmaceutical Co,.Ltd
Tel
86-0531-81263406
Fax
86-0531-58591634
Email
sales@aerpharm.com
Country
China
ProdList
66
Advantage
55
Shanghai Boyle Chemical Co., Ltd.
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2926
Advantage
55
J & K SCIENTIFIC LTD.
Tel
400-666-7788 +86-10-82848833
Fax
86-10-82849933
Email
jkinfo@jkchemical.com;market6@jkchemical.com
Country
China
ProdList
96815
Advantage
76
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
86-21-50328103 * 801、802、803、804 Mobile:18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15881
Advantage
69
ZHIWE CHEMTECH CO LTD
Tel
021-20221225;13917446399;QQ:2381298399
Email
sales@zhiwe.net;zwchem@163.com
Country
China
ProdList
469
Advantage
61
Chembest Research Laboratories Limited
Tel
+86(0)21-20908456
Fax
+86(0)21-58180499
Email
sales@biochembest.com; market@biochembest.com
Country
China
ProdList
5996
Advantage
61
TCI (Shanghai) Development Co., Ltd.
Tel
021-67121386 / 800-988-0390
Fax
021-67121385
Email
Sales-CN@TCIchemicals.com
Country
China
ProdList
24555
Advantage
81
Capot Chemical Co., Ltd
Tel
+86 (0) 571 85 58 67 18
Fax
0086-571-85864795
Email
sales@capotchem.com
Country
China
ProdList
18228
Advantage
66
Jia Xing Isenchem Co.,Ltd
Tel
0573-85280080,18627885956
Fax
0573-85285100
Email
isenchem@163.com,QQ:2446116053
Country
China
ProdList
9729
Advantage
66
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View Lastest Price from Nepafenac manufacturers

career henan chemical co
Product
Nepafenac 78281-72-8
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-23
career henan chemical co
Product
Nepafenac 78281-72-8
Price
US $7.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-21
career henan chemical co
Product
Nepafenac 78281-72-8
Price
US $7.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-21

78281-72-8, NepafenacRelated Search:


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