Drugs online research references
Inflammation. 2000 Aug;24(4):357-70.
Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy.
Gamache DA, Graff G, Brady MT, Spellman JM, Yanni JM.
Pharmaceutical Products Research, Alcon Research, Ltd., Fort Worth, Texas, USA.
Nepafenac, the amide analog of 2-amino-3-benzoylbenzeneacetic acid (amfenac), was examined in preclinical models for its potential utility as a topical ocular anti-inflammatory agent. Diclofenac was selected as the reference compound. In contrast to diclofenac (IC50 = 0.12 microM), nepafenac exhibited only weak COX-1 inhibitory activity (IC50 = 64.3 microM). However, amfenac was a potent inhibitor of both COX-1 (IC50 = 0.25 microM) and COX-2 activity (IC50 = 0.15 microM). Ex vivo, a single topical ocular dose of nepafenac (0.1%) inhibited prostaglandin synthesis in the iris/ciliary body (85-95%) and the retina/choroid (55%). These levels of inhibition were sustained for 6 h in the iris/ciliary body and 4 h in the retina/choroid. Diclofenac (0.1%) suppressed iris/ciliary body prostaglandin synthesis (100%) for only 20 min, with 75% recovery observed within 6 h following topical dosing. Diclofenac's inhibition of prostaglandin synthesis in the retina/choroid was minimal. Nepafenac's inhibitory efficacy and longer duration of action was confirmed in a trauma-induced rabbit model of acute ocular inflammation monitoring protein or PGE2 accumulation in aqueous humor. Results warrant further assessment of nepafenac's topical ocular efficacy in the treatment of postoperative ocular pain, inflammation, and posterior segment edema.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10850857&dopt=Abstract
Inflammation. 2000 Aug;24(4):371-84.
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.
Ke TL, Graff G, Spellman JM, Yanni JM.
Pharmaceutical Products Research, Alcon Research, Ltd. Fort Worth, Texas, USA.
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.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10850858&dopt=Abstract
Curr Med Res Opin. 1982;7(Suppl 1):41-52.
Osteoarthritis and non-steroidal and anti-inflammatory drugs: a multi-centre comparative study.
Pathy MS.
An open, multi-centre study was carried out in 239 elderly out-patients referred with symptomatic osteoarthritis of the hip and/or knee to assess the effectiveness of 200 mg sulindac twice daily compared with either 400 mg ibuprofen 3-times daily, 250 mg naproxen twice daily or 25 mg diclofenac 3-times daily. Assessments were made before and during the 12-week trial period of disease activity, weight-bearing pain, pain on active and passive movement, night pain, and inactivity stiffness. The results showed that there was significant improvement in all of the parameters with each of the treatments, and the difference between treatments was significant in favour of sulindac compared with ibuprofen in disease activity, weight-bearing pain and pain on active movement. In the overall assessment of response to treatment at the end of the trial it was the patients' opinion that the degree of improvement was better on sulindac than on the comparative drugs. The main side-effect leading to some patients withdrawing from the trial was abdominal pain.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7105795&dopt=Abstract
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