Journal Article10.1023/A:1007001131987
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
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TL;DR: The enhanced permeability of nepafenac, combined with rapid bioactivation to amfenac by the iris/ciliary body and retina/choroid, make it a target specific NSAID for inhibiting prostaglandin formation in the anterior and posterior segments of the eye.
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Abstract: Nepafenac, the amide analog of the NSAID amfenac, was examined in vitro for its bioactivation by ocular tissue components and its ability to permeate external ocular barriers. Rabbit tissues catalyzed a concentration-dependent conversion of nepafenac to amfenac. The order of specific hydrolytic activity is retina/choroid >> iris/ciliary body. Corneal tissue showed only minimal activity. Similarly, in human ocular cadaver tissue the specific activity of iris/ciliary body was greater than cornea. Continued perfusion of the corneal epithelium demonstrated a nearly six-fold greater permeation coefficient for nepafenac (k(p) = 727 x 10(-6) min(-1)) than for diclofenac (k(p) = 127 x 10(-6) min(-1)). Superior permeation of conjunctival and scleral tissue by nepafenac (k(p) = 128 x 10(-6) min(-1)) compared to diclofenac (k(p) = 80 x 10(-6) min(-1)) was also evident. Short term perfusion (5 min) of the corneal surface with 0.1% nepafenac resulted in sustained flux of drug across the cornea for 6 h. Under identical conditions only 3.3 microM of diclofenac accumulated on the corneal endothelial side compared to 16.7 microM nepafenac. The enhanced permeability of nepafenac, combined with rapid bioactivation to amfenac by the iris/ciliary body and retina/choroid, make it a target specific NSAID for inhibiting prostaglandin formation in the anterior and posterior segments of the eye.
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Citations
Therapeutic Drugs for Anterior Segment Ocular Surgery
Malik Y. Kahook,Joel S. Schuman +1 more
- 01 Jan 2008
TL;DR: This chapter provides an account for the therapeutic drugs for anterior segment ocular surgery, with four classes of ophthalmic medications that predominate: Non-Steroidal Anti-Inflammatory Drugs (NSAIDs); steroids; antibiotics; and (4) topical ocularmic anesthetics.
Dirençli diyabetik makula ödemi tedavisinde kombine intravitreal triamsinolon – bevacizumab ile topikal nepafenak tedavisinin kısa dönem etkisi
Handan Bardak,Murat Gunay,Yavuz Bardak,Mustafa Muhterem Ekim +3 more
- 01 Mar 2016
TL;DR: The short term effect of combined intravitreal triamcinolone acetonide (IVTA) and bevacizumab (IVB) injection with topical nepafenak, triamsinolon asetonid in REFRACTORY DIABETIC MACULAR EDEMA SUMMARY was investigated.
An Interventional Follow up Study to Determine the Effect of Nepafenac 0.1% in Macular thickness in Patients who had Undergone Cataract Surgery as Determined By OCT
Rama Vadapalli,Vankadara Naga Suresh +1 more
- 31 Oct 2016
TL;DR: The aim of the study is to determine the role of Nepafenac 0.1% usage in altering the status of CME as determined by OCT who underwent Cataract Surgery.
Differences in pain and inflammation between Diclofenac 0.1% and Nepafenac 0.1% after cataract surgery
Ika Nuraita,Retno Ekantini,Rinanto Prabowo,Suhardjo Pawiroranu,Agus Supartoto,Indra Tri Mahayana +5 more
- 28 Dec 2020
TL;DR: The pain and flare-cell levels in Nepafenac group are lower when compared with Diclofenacgroup, according to a prospective randomized clinical trial conducted in patients undergoing cataract surgery.
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