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Ocular anti‐inflammatory activity of amfenac relative to other nonsteroidal anti‐inflammatory agents
Author(s) -
Waterbury L. David
Publication year - 2006
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.20.5.a1127-c
Subject(s) - ketorolac , diclofenac , pharmacology , anti inflammatory , drug , medicine , inflammation , diclofenac sodium , dextran , nonsteroidal , analgesic , chemistry , immunology , chromatography
Purpose To determine the ocular anti‐inflammatory activity of amfenac in a rabbit model of inflammation. Nepafenac, a pro‐drug of amfenac, has recently been approved as an ocular anti‐inflammatory drug. Amfenac is structurally similar to diclofenac, and nearly identical to bromfenac. Both amfenac and bromfenac are potent COX‐2 inhibitors. Methods In this study, amfenac 0.1%, ketorolac 0.4%, diclofenac 0.1%, bromfenac 0.1% or vehicle were administered in 2, 50 μL doses to New Zealand white rabbits. Endotoxin was then given to induce ocular inflammation. Changes in the blood‐aqueous barrier were determined by FITC‐dextran fluorophotometry. Results Amfenac 0.1% resulted in a nearly complete inhibition (97.4%) of FITC‐dextran leakage into the anterior chamber. A similar degree of inhibition was seen with ketorolac 0.4% (98.7% inhibition) and bromfenac (99.4% inhibition). Diclofenac 0.1% was significantly less active in inhibiting the inflammatory response. Conclusions The marked inhibition of endotoxin‐induced FITC‐dextran leakage seen with amfenac in this study is consistent with its potent COX‐2 inhibition, and suggests that the pro‐drug form of nepafenac is not required for ocular absorption or activity. Amfenac showed greater anti‐inflammatory activity in this study than has been reported for nepafenac in similar animal models.