Nepafenac-d5 is intended for use as an internal standard for the quantification of nepafenac by GC- or LC-MS. Nepafenac is a prodrug form of amfenac, a non-steroidal anti-inflammatory drug (NSAID) and an inhibitor of COX-1 and COX-2.1 Nepafenac is an inhibitor of prostaglandin (PG) synthase 1 (IC50 = 64.3 ?M) that inhibits the production of PGs in isolated rabbit iris/ciliary body.2 It also reduces protein and PGE2 accumulation in a rabbit model of acute ocular inflammation when applied topically at a concentration of 0.1% prior to paracentesis. Formulations containing nepafenac have been used in the treatment of pain and inflammation associated with cataract surgery.
1.Gamache, D.A., Graff, G., Brady, M.T., et al.Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacyInflammation24(4)357-370(2000) 2.Ke, T.L., Graff, G., Spellman, J.M., et al.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 barriersInflammation24(4)371-384(2000)