Comparison of Ketorolac Tromethamine, Diclofenac Sodium, and Loteprednol Etabonate in an Animal Model of Ocular Inflammation
The aim of this study was to compare the anti-inflammatory activities of ketorolac tromethamine 0.4% and 0.1%; diclofenac sodium 0.1%; and loteprednol etabonate 0.5% suspension in an animal model of ocular inflammation.
An ocular inflammatory response was induced in New Zealand White rabbits by the intravenous (i.v.) administration of 10 microg/kg lipopolysaccharide (LPS). In study animals, 1 eye was treated topically with 50 microL of study medication (n = 8 animals per drug) and the other eye was treated topically with a 50-microL vehicle (buffered saline). In control animals (n = 8), both eyes were treated with vehicle. All animals were treated twice: 2 h and 1 h before LPS challenge. The breakdown of the blood-aqueous barrier in the anterior chamber was measured by fluorophotometry (FITC-dextran 30 mg/kg, i.v. given immediately after LPS challenge). Aqueous prostaglandin E(2) (PGE(2)) levels were measured using an enzyme-linked immunosorbent assay (ELISA) immunoassay.
Ketorolac 0.4% resulted in a nearly complete inhibition of endotoxin-induced increases in FITC-dextran and PGE(2) synthesis (P < 0.001 vs. vehicle). Diclofenac 0.1% had much less of an effect on these parameters (P < 0.01 vs. ketorolac 0.4%). Loteprednol 0.5% was no more effective than vehicle at inhibiting increases in FITC-dextran.
Ketorolac has greater anti-inflammatory effects than diclofenac and loteprednol.
Available from: PubMed Central
- "Waterbury and Flach (Waterbury and Flach 2006) using a rabbit model of ocular inflammation induced by injecting a lipopolysaccharide endotoxin isolated from Salmonella enterica intravenously investigated the anti-inflammatory activity of ketorolac 0.4% and other NSAIDs. They reported a nearly complete inhibition of PG synthesis in the aqueous humor compared with vehicle. "
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ABSTRACT: The non-steroidal anti-inflammatory drug (NSAID) ketorolac tromethamine 0.4% ophthalmic solution, a recent reformulation containing 20% less active ingredient that the original formulation, is indicated for the reduction of ocular pain and burning/stinging following corneal refractive surgery. Clinical studies have shown ketorolac tromethamine 0.4% to be as effective as ketorolac tromethamine 0.5% to control inflammation after cataract surgery including prevention of cystoid macular edema (CME). Its efficacy to inhibit miosis during cataract surgery as well as its role in the treatment of dry eye has been reported. The purpose of this paper is to review the use of ketorolac tromethamine 0.4% in the treatment of post-surgical inflammation following cataract and refractive surgery.
Available from: Rachel A Allbaugh
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ABSTRACT: Objective – To measure blood aqueous-barrier breakdown following aqueocentesis using various needle sizes and to monitor the intraocular pressure (IOP) response. Animals – 24 healthy, adult dogs received treatment (24 treated eyes, 24 contralateral eyes); 3 dogs were untreated controls (6 control eyes). Procedures – Dogs receiving treatment were divided into 3 equal groups (25-, 27-, or 30- gauge needle aqueocentesis). In each dog the treated eye was determined randomly, the contralateral eye was untreated. Dogs that did not have aqueocentesis performed in either eye were used as controls. Aqueocentesis at the lateral limbus was performed under sedation and topical anesthesia. Anterior chamber fluorophotometry was performed before and after aqueocentesis on day 1. On days 2-5 sedation and fluorophotometry were repeated. Intraocular pressure was measured with a rebound tonometer at multiple time points. Results – Aqueocentesis resulted in blood-aqueous barrier breakdown in all treated eyes with barrier reestablishment present by day 5 detected by fluorophotometry. On day 2 the contralateral untreated eyes of all groups also showed statistically significant increased fluorescence (P < 0.05) following treatment of the opposite eye, but these values were not statistically significantly greater than untreated controls. In treated eyes there was no statistical difference in fluorescein concentration or IOP between 27- and 30-gauge needles. Use of the 25- gauge needle resulted in a statistically significant increase in anterior chamber fluorescence on days 3 and 5. It also caused a statistically significant increase in IOP 20 minutes following aqueocentesis as compared to the 27- and 30-gauge needles. Aside from this transient ocular hypertension, rapid resolution of ocular hypotony following aqueocentesis was observed in all treatment groups. Conclusions and Clinical Relevance – Aqueocentesis using a 25-gauge needle resulted in a greater degree of blood-aqueous barrier breakdown and a brief state of intraocular hypertension following paracentesis. Use of a 27- or 30-gauge needle is recommended for aqueous paracentesis. A consensual ocular reaction appeared to occur in dogs following unilateral traumatic blood-aqueous barrier breakdown and may be of clinical significance. Statistical significance was limited in this study due to high variability and large standard deviations. Kansas State University College of Veterinary Medicine Mentored Clinical, Applied or Translational Research Grant Master of Science Masters Department of Clinical Sciences Amy J. Rankin
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ABSTRACT: A range of diclofenac salts was prepared with a variety of alkyl, hydroxyalkyl and alkyl hydroxyalkyl linear amines, and characterized by thermal analysis (DSC, TGA, and HSM). Another seven similar salts, previously described, were also prepared for a more careful analysis and comparison. The aim of this paper is a deeper knowledge of this class of compounds, previously poorly examined and that have, on the contrary, proved to offer complex situations in the solid state, as resulted by thermal analysis. The whole class of these salts presents a variety of behaviours, ranging from the formation of hydrates to polymorphs and hydrate polymorphs in the solid state. The salts with diethanolamine, triethanolamine, N-ethyl monoethanolamine and TRIS bases crystallize anhydrous. All the salts demonstrated thermal instability at temperature above the melting point, showing a dramatic loss of weight. In each case the TGA profile indicates that it corresponds to the base content inside the salt: this event is associated with a broad endotherm in the DSC thermogram that follows or overlaps with that of the melting endotherm. Prolonged heating in the oven of salts with very volatile amines causes decomposition, even at low temperatures, leaving the starting acidic diclofenac as residue. Different phases, in the case of polymorphs, were revealed, registering melting/re-crystallization by hot stage microscopy, as in the case of the salts with triethylamine and N-methyl monoethanolamine; while in the case of the salt with monoethanolamine evidence was obtained by means of DSC. The relationship between the structure of the starting bases and solid-state nature of these diclofenac salts studied is briefly discussed.
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