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Pharmacokinetic-Pharmacodynamic Correlations of Corticosteroids
Published in Hartmut Derendorf, Günther Hochhaus, Handbook of Pharmacokinetic/Pharmacodynamic Correlation, 2019
Helmut Möllmann, Stefan Baibach, Günther Hochhaus, Jürgen Barth, Hartmut Derendorf
Rimexolone (RIM) is used in local therapy of rheumatoid arthritis.129 Intra-articular administration of RIM crystal suspensions into the knee joint provides a sustained release over a period of 3 months due to the extremely poor solubility of this lipophilic compound in aqueous media.130 The disposition is absorption-limited (“flip-flop-case”) and dose-independent. A total body clearance of 106 l/h and a Vd of 116 l were found after intra-articular treatment. In comparison to other corticosteroids utilized for this route of administration, RIM has an extremely long MRT of 25 d. In addition, RIM has a high receptor affinity.131,132 These facts indicate that the duration of effect exceeds those of other drugs investigated such as TCA, BET, MP, and their derivatives, dramatically.25,26
Difluprednate 0.05% versus Prednisolone Acetate 1% for Endogenous Anterior Uveitis: Pooled Efficacy Analysis of Two Phase 3 Studies
Published in Ocular Immunology and Inflammation, 2019
John D. Sheppard, C. Stephen Foster, Melissa M. Toyos, Kerry Markwardt, Robert Da Vanzo, Thomas E. Flynn, John H. Kempen
The results of this post-hoc pooled analysis further support the findings of the individual studies. Both study designs designated the result at 14 days as the primary outcome, at which point there were not statistically significant differences between groups for the primary endpoint. However, notable differences favored difluprednate regarding withdrawal from study due to inefficacy, and better inflammatory sign outcome at 21 days. These observations as well as the observation that the mean improvement from baseline in AC cell grade was numerically greater with difluprednate at all time points except on day three, suggest that difluprednate may have greater potency. The two treatment groups were similar in terms of other inflammatory and QOL markers. Effective inflammation control of anterior uveitis is essential because under-treatment can lead to vision-related complications and ultimately vision loss.17 Rimexolone is another topical steroid observed in randomized trials to be clinically and statistically equivalent to prednisolone acetate in controlling uveitic inflammation.18,19 Other topical steroids shown in previous randomized trials to be effective in the treatment of anterior uveitis are betamethasone phosphate, clobetasone butyrate, hydrocortisone, loteprednol etabonate, and tolmetin sodium dihydrate.20–24
The Use of Topical Corticosteroids for Treatment of Dry Eye Syndrome
Published in Ocular Immunology and Inflammation, 2019
Carlo Alberto Cutolo, Stefano Barabino, Chiara Bonzano, Carlo Enrico Traverso
Rimexolone is a highly lipophilic corticosteroid that lacks a hydroxyl group at the 21 position. Several studies have shown that rimexolone has minimal effects on IOP, whereas its efficacy in reducing inflammation is similar to that of prednisolone acetate 1%.66,67 Rimexolone is commercially available in some countries as 1% ophthalmic suspension and is approved by the FDA for the treatment of postoperative inflammation after ocular surgery and the treatment of anterior uveitis. A Phase II RCT has been conducted to evaluate the safety and effectiveness of rimexolone for the treatment of DED.C The results of the trial have not yet been published.