Product Name

Nepafenac

Name: Nepafenac - LGM Pharma
SKU: 78281-72-8

CAS Number

78281-72-8

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Product Name:

Nepafenac

CAS Number:

78281-72-8

Indication:

For the treatment of pain and inflammation associated with cataract surgery.

Mode of Action:

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.

Pharmacodynamics:

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.

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.

Toxicity:

Ocularly applied non-steroidal anti-inflammatory drugs may cause increased bleeding of ocular tissues (including hyphemas) in conjunction with ocular surgery.

IUPAC:

Benzeneacetamide, 2-amino-3-benzoyl-

ATC:

S01BC10

PubChem:

151075

DrugBank:

DB06802

Formula:

C15-H14-N2-O2

Molecular Mass:

254.288

Synonyms:

2-(2-Amino-3-benzoylphenyl)acetamide, 2-Amino-3-benzoylbenzeneacetamide, AHR 9434, AHR-9434, AL 6515, AL-6515, Ilevro, Nepafenac, Nevanac, UNII-0J9L7J6V8C

SMILES:

c1ccc(C(=O)c2c(c(ccc2)CC(N)=O)N)cc1

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)

General Reference:

Gamache DA, Graff G, Brady MT, Spellman JM, Yanni JM: Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy. Inflammation. 2000 Aug;24(4):357-70. Pubmed
Ke TL, Graff G, Spellman JM, Yanni JM: Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: II. In vitro bioactivation and permeation of external ocular barriers. Inflammation. 2000 Aug;24(4):371-84. Pubmed
Lane SS, Modi SS, Lehmann RP, Holland EJ: Nepafenac ophthalmic suspension 0.1% for the prevention and treatment of ocular inflammation associated with cataract surgery. J Cataract Refract Surg. 2007 Jan;33(1):53-8. Pubmed
Walters T, Raizman M, Ernest P, Gayton J, Lehmann R: In vivo pharmacokinetics and in vitro pharmacodynamics of nepafenac, amfenac, ketorolac, and bromfenac. J Cataract Refract Surg. 2007 Sep;33(9):1539-45. Pubmed
Bucci FA Jr, Waterbury LD: Re: Pharmacokinetics and pharmacodynamics of nepafenac, amfenac, ketorolac, and bromfenac. J Cataract Refract Surg. 2008 Aug;34(8):1226; author reply 1226-7. Pubmed
Summary Basis of Decision (SBD): NEVANAC. Health Canada

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Nepafenac

78281-72-8

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