Outcome and risk of ocular complications of managing children with chronic anterior uveitis with topical rimexolone 1.

PURPOSE: To investigate the efficacy and safety of 1% rimexolone ophthalmic suspension in children with chronic anterior uveitis under real-life conditions in a tertiary center. METHODS: This is a retrospective longitudinal study. Medical records were analyzed at baseline, 1, 3, 6 and 12 months before and after switching to rimexolone for best-corrected visual acuity (BCVA), oral steroid use, number of flares, IOP and anti-glaucoma management. RESULTS: Twenty-four patients (41 eyes) diagnosed with either anterior uveitis (n = 25, 60.0%) or panuveitis (n = 16, 40%) were enrolled. The mean age was 10.5 years (4-16 years). The number of patients requiring oral prednisolone reduced from 8 patients (32.0%) at baseline to 3 patients (20.0%) at 12 months (P < 0.001). Following baseline, the median number of uveitis flares reduced from 2.0 (inter-quartile range (IQR) 1.0-2.75) to 1.0 (IQR 0.0-1.0) compared to the 12 months before baseline (P < 0.001). The mean IOP reduced from baseline (22.0 ± 7.3 mmHg) to 1 month (18.8 ± 8.7 mmHg, P = 0.01) and remained stable up to 12 months (15.9 ± 5.0 mmHg, P < 0.001). Average BCVA, dose of oral prednisolone and anti-glaucoma treatments did not change compared to the baseline. The development for IOP ≥ 30 mmHg was associated with a known corticosteroid response [odds ratio (OR) 6.8, P = 0.003] and a dose > 7.5 mg/day oral prednisolone (OR 4.4, P = 0.033). CONCLUSIONS: Rimexolone 1% ophthalmic suspension is an effective and safe topical steroid for pediatric anterior uveitis.

Retrospective analysis of a single-center clinical experience toward development of curative treatment of 123 pemphigus patients with a long-term follow-up: efficacy and safety of the multidrug protocol combining intravenous immunoglobulin with the cytotoxic immunosuppressor and mitochondrion-protecting drugs.

BACKGROUND: Pemphigus vulgaris (PV) is a life-long IgG autoantibody-mediated blistering disease affecting the mucosal surfaces lined by the stratified epithelium (oral, nasal, genital) and sometimes also the skin. While corticosteroid treatment is life saving, the high dose and prolonged courses required for disease control are associated with significant adverse effects, including death. Although introduction of rituximab (RTX) provided for a favorable outcome, the high relapse rate, that is, up to 80%, precludes successful use of RTX as a monotherapy. Intravenous immunoglobulin (IVIg) is being increasingly utilized as off-label therapy for a variety of autoimmune and inflammatory diseases, including PV and pemphigus foliaceus (PF). AIMS: The goal of pemphigus research is to develop an effective treatment modality that would allow patients to achieve and maintain a stable clinical remission without the need for additional treatments, or cure. MATERIALS AND METHODS: This article summarizes clinical outcome of 123 pemphigus patients treated with a combination of IVIg, an immunosuppressive cytotoxic drug (ICD) and mitochondrion-protecting drugs in the Blistering Disease Clinic at the University of California, Irvine from 2007 to 2017. RESULTS: The mean time to disease control was 0.2 months and time to complete remission - 1.7 months. Duration of complete remission on drugs until relapse or end of treatment was 19.3 months. The mean duration of complete remission off drugs until relapse was 15.8 months. That until end of follow up was 48.4 months, with a minimum of 14 and a maximum of 91 months. The overall complete remission rate off all drugs was 100%, with 12% overall relapse rate. Most relapses, 8.1 vs. 3.3%, occurred during the time of treatment, compared to posttreatment. No patients had more than a single relapse. The duration of the posttreatment follow-up ranged from 9 to 97 months with a mean of 64.8 months, or 5.4 years. The total number of IVIg cycles ranged from 26 in patients without a relapse to 37 in patients with a relapse. The clinical outcome in patients that received IVIg with RTX or another ICD were found to be very similar. DISCUSSION: Thus, the multidrug IVIg regimen allowed to achieve three principal treatment objectives: (i) rapid control of pemphigus symptoms; (ii) stable disease remission; and (iii) overall safety of treatment. CONCLUSIONS: While the individualized therapeutic approaches to eradicate the autoreactive B cell clones causing disease in each particular PV or PF patient are being developed, all pemphigus patients can benefit from the treatment protocol described in this study.

Steroid-induced ocular hypertension in the pediatric age group.

PURPOSE: Comparing the effects of topical Rimexolone versus Dexamethasone and Rimexolone versus Fluorometholone on the intraocular pressure in children <13 years. METHODS: A total of 40 patients (80 eyes) undergoing bilateral recession strabismus surgery were divided into two groups. Group A included 20 children (40 eyes); for each, one eye was randomized to receive 1% Rimexolone and the fellow eye received 0.1% Dexamethasone. Group B included 20 children (40 eyes); for each, one eye was randomized to receive 1% Rimexolone and the fellow eye received 0.1% Fluorometholone. Patients received eye drops for two consecutive weeks. Preoperative and postoperative intraocular pressure values for weeks 1, 2, 3, 4, and 6 were measured. The ocular-hypertensive response of all patients was categorized as either high, intermediate or low (Armaly-Becker Classification). RESULTS: After a 2-week treatment for both groups, peak and maximal intraocular pressure changes were reached. Changes were significantly higher in the Dexamethasone-treated eyes than in the Rimexolone- and Fluorometholone-treated eyes, which had a comparable change. (Week 2 intraocular pressure Group A: 14.15 ± 3.23 mmHg vs 17.95 ± 4.27 mmHg; Group B: 15.1 ± 2.27 mmHg vs 15.2 ± 2.73 mmHg). In both groups, the increase was statistically significant compared to the baseline intraocular pressure (preoperative intraocular pressure Group A: 13.2 ± 3.53 mmHg vs 13.1 ± 3.43 mmHg; Group B: 12.55 ± 2.98 mmHg vs 12.15 ± 3.31 mmHg). Intraocular pressure returned to near preoperative values over the following four consecutive weeks (Week 6 intraocular pressure Group A: 12.25 ± 2.67 mmHg vs 12.55 ± 2.95 mmHg; Group B: 12.15 ± 2.8 mmHg vs 12.00 ± 2.75 mmHg). None of the patients were high responders. CONCLUSION: Dexamethasone caused a higher elevation in intraocular pressure than Rimexolone and Fluorometholone in children. The ocular-hypertensive response was transient after the 2-week course.

Effect of combined topical heparin and steroid on corneal neovascularization in children.

BACKGROUND AND OBJECTIVE: To demonstrate the effect of topical heparin combined with topical steroid on corneal neovascularization (CN) in children. PATIENTS AND METHODS: Four children (5 eyes) with new-onset progressive CN in at least one eye received topical rimexolone or dexamethasone in combination with heparin until complete regression of CN was obtained. The regression of CN was documented by slit-lamp or anterior segment photography. RESULTS: All 5 eyes showed complete regression of CN within 5 months. An anti-angiogenic effect was found as early as 1 week after starting topical combination treatment. No ocular and systemic side effects were detected and treatment was well tolerated by all children. In the 3 eyes with involvement of the optical axis, symmetrical visual acuity was obtained by amblyopia treatment. Recurrence of the CN was detectable in 2 eyes at 1 and 6 months, respectively, after ending combination therapy. Both eyes responded favorably to re-treatment. CONCLUSION: Combination of topical heparin and steroid leads to rapid regression and complete inactivity of CN. This therapeutic approach is promising, especially in children with limited therapeutic alternatives and a high risk for amblyopia.

Do topical ophthalmic corticosteroids suppress the hypothalmic-pituitary-adrenal axis in post-penetrating keratoplasty patients?

PURPOSE: To establish whether hypothalmic-pituitary-adrenal axis suppression is possible secondary to long-term topical ophthalmic corticosteroid use in patients who have undergone penetrating keratoplasty (PKP). METHODS: Patients who had undergone a PKP and had been using corticosteroid-based eye drops continuously for more than 6 months, with no history of concomitant steroid (oral, inhaled, or cutaneous) use, were included within the study. A low-dose short Synacthen (LDSST) test was performed in each patient followed later by a short Synacthen test (SST). The mean SST and LDSST after 30 min were calculated along with their corresponding 95% confidence intervals (CIs). Correlation between both baseline SST and baseline LDSST with duration of treatment was determined using Spearman's correlation. RESULTS: In all, 20 patients were included within the study. The mean duration treatment was 28.2 months (range 11-96 months). All patients had normal baseline cortisol levels in both SST and LDSST tests. The mean 30 min SST was 753.8 nmol/l (95%CI: 696.6 nmol/l, 811.0 nmol/l) and no patients displayed inadequate adrenal response. The mean 30 min LDSST was 709.8 nmol/l (95%CI: 665.1 nmol/l, 754.5 nmol/l) and only one patient had an inadequate adrenal response. There was no correlation between baseline SST or LDSST and duration of treatment. CONCLUSIONS: This study found no evidence that patients using continuous long-term corticosteroid eye drops after PKP experienced inadequate adrenal response. We did not find any evidence of a negative correlation between length of treatment and SST or LDSST measurements at baseline.

Risk of cataract development among children with juvenile idiopathic arthritis-related uveitis treated with topical corticosteroids.

PURPOSE: We sought to investigate the risk of cataract development among patients with juvenile idiopathic arthritis (JIA)-associated uveitis treated with topical corticosteroids. DESIGN: Retrospective cohort study. PARTICIPANTS: We included 75 patients with JIA-associated uveitis observed from July 1984 through August 2005 at a single academic center. METHODS: Clinical data on these patients were collected by chart review and were analyzed. MAIN OUTCOME MEASURES: Incidence of new-onset cataract. Risk factors for cataract development were assessed with attention paid to the use of topical corticosteroids. RESULTS: Over a median follow-up of 4 years, the incidence of new-onset cataract was 0.04/eye-year (EY; 95% confidence interval [CI], 0.02-0.09). Of the 60 eyes in 40 patients who received topical corticosteroid therapy, there was a dose-dependent increase in the rate of cataract development among eyes receiving topical corticosteroids. The incidence of cataract was 0.01/EY for eyes treated with < or = 3 drops daily and 0.16/EY (P = 0.0006 for log-rank test) for eyes treated with >3 drops daily. Among eyes receiving < or = 2 drops daily, the incidence of cataract was 0/EY (95% CI [1 sided], 0.03/EY). Presence of posterior synechiae, active uveitis, and use of topical corticosteroids at presentation were significantly associated with cataract development after controlling for confounding variables. Use of topical corticosteroids was associated with cataract formation independent of uveitis activity. Using longitudinal data analysis and controlling for duration of uveitis, presence and degree of active uveitis, and concomitant use of other forms of corticosteroids in a time-updated fashion, treatment with < or = 3 drops daily of topical corticosteroid was associated with an 87% lower risk of cataract formation compared with eyes treated with >3 drops daily (relative risk, 0.13; 95% CI, 0.02-0.69; P = 0.02). CONCLUSIONS: In our cohort, topical corticosteroid use was associated with an increased risk of cataract formation independent of active uveitis or presence of posterior synechiae. However, chronic use of topical corticosteroids dosed at < or = 3 drops daily seemed to be associated with a lower risk of cataract development relative to eyes receiving higher doses over follow-up in the setting of suppressed uveitis. FINANCIAL DISCLOSURE(S): Proprietary or commercial disclosure may be found after the references.

[0.1% dexamathasone and 1% rimexolone. A comparative study in the postoperative treatment after cataract extraction]. / Dexametasona al 0,1% versus rimexolona al 1%. Estudio comparativo en el postoperatorio de la cirugía de cataratas.

PURPOSE: To compare the efficiency and secondary effects of using 1% rimexolone or 0.1% dexamethasone as postoperative treatment for cataract surgery. MATERIALS AND METHODS: A prospective study performed on a cohort of 37 patients undergoing cataract surgery by phacoemulsification with no intraoperative complications at the Hospital Clínico San Carlos, Madrid. After surgery, 19 of the patients were randomly assigned to receive topical 0.1% dexamethasone (DEX group) as inflammatory treatment and the remaining 18 subjects were treated with 1% rimexolone ( RIMEX group) following the same regime. Twenty four hours and one month after surgery, visual acuity, conjunctival hyperaemia, anterior chamber cells, anterior chamber flare, intraocular pressure, corneal thickness and macular edema were determined in each patient. RESULTS: The repeated measures test performed on 24 hours and 1 month data revealed a significant difference between the two treatments in terms of Tyndall (p = 0.001) and flare (p= 0.034) values; these variables being lower in the dexamethasone group. No differences were observed in the remaining variables examined. CONCLUSIONS: Rimexolone is as efficient and safe as dexamethasone for the treatment of patients undergoing cataract extraction.

Rimexolone 1% versus prednisolone acetate in preventing early postoperative inflammation after cataract surgery.

PURPOSE: To compare the efficacy and safety of rimexolone 1% and prednisolone acetate 1% ophthalmic suspensions in controlling intraocular inflammation in the early period after cataract surgery. METHODS: Eighty patients undergoing cataract extraction with intraocular lens implantation, either planned extra capsular cataract extraction (PECCE) or phacoemulsification surgery, were evaluated in a prospective, randomized, observer-masked, clinical trial in which efficacy in controlling early postoperative inflammation and safety of prednisolone acetate 1% one eye drop every 4 h (n = 36 eyes) was compared with that of rimexolone 1% one eye drop every 4 h (n = 44 eyes) in an eighteen day course. Efficacy was assessed from changes of the anterior chamber cell count, flare, conjunctival hyperemia, and ciliary congestion by means of slit lamp biomicroscopy on days 1, 3, 8, 15, and 18. Intraocular pressure (IOP) and possible side effects were also recorded on each visit. RESULTS: Anterior chamber cell count and flare showed no difference in the two groups at any visits. The rimexolone group was associated with significantly higher score for conjunctival hyperemia on days one and three (P < 0.05) and the prednisolone acetate group was associated with a significantly higher score for corneal edema on day 8 (P < 0,05). However, there were no between group differences in IOP. CONCLUSIONS: Rimexolone 1% ophthalmic suspension was as effective and safe as prednisolone acetate 1% ophthalmic suspension in controlling inflammation in the early period after cataract surgery.

Comparison of prednisolone 1%, rimexolone 1% and ketorolac tromethamine 0.5% after cataract extraction: a prospective, randomized, double-masked study.

PURPOSE: To compare the efficacy, safety and patient comfort of two topical steroids (prednisolone 1% and rimexolone 1%) and a topical non-steroidal anti-inflammatory agent (ketorolac tromethamine 0.5%) after extracapsular cataract extraction. METHODS: Forty-five patients were enrolled in this prospective, randomized, double-blind study. They were assigned to receive topical treatment with either prednisolone, rimexolone or ketorolac tromethamine ophthalmic solution after phacoemulsification for cataract extraction. On postoperative days 1, 3, 5, 14 and 28 best-corrected visual acuity, intraocular pressure (IOP), slit-lamp examination of the anterior segment and report of the patients' comfort were assessed and compared by Friedman rank time analysis. RESULTS: Regarding the primary outcome efficacy of inflammation control the assessment of cells did not differ (p=0.165), while flare in the anterior chamber was lowest (p=0.008) in the non-steroidal anti-inflammatory drug (NSAID) group. Surface inflammation was lowest with prednisolone (p=0.002). Regarding safety, visual acuity did not differ among the groups. In the prednisolone group one patient, however, responded to steroid treatment with elevated IOP and had to be excluded. In the remaining patients IOP was even lower in the two steroidal treatment groups than with ketorolac (p=0.030). One patient receiving ketorolac had to be excluded because a corneal erosion developed. Patient comfort was highest with prednisolone (p=0.041). CONCLUSIONS: Ketorolac tromethamine provides good control of intraocular inflammation after cataract extraction without the risk of a steroidal IOP increase, which was also not observed under rimexolone therapy. The best surface inflammation control and patient comfort was observed with prednisolone, which remains a good choice.

Ocular-hypertensive and anti-inflammatory response to rimexolone therapy in children.

OBJECTIVE: To compare the ocular-hypertensive and anti-inflammatory response to rimexolone (116-hydroxy-16alphafluoro-6alphamethylpresdnisolone) and fluorometholone (21-deoxy-9alphafluoro-6alphamethylprednisolone) therapy in children's eyes. METHODS: With parental consent, children who underwent surgical procedures for bilateral symmetric strabismus from January 18, 2000, through November 16, 2001, were recruited. One eye was randomized to receive topical 1% rimexolone while the contralateral eye received topical 0.1% fluorometholone, 4 times daily for 4 weeks. MAIN OUTCOME MEASURES: Intraocular pressures and anti-inflammatory responses were the main outcome measures and were serially measured postoperatively for 8 weeks. RESULTS: Fifty-four children, aged from 4 to 8 years (mean [SD] age, 5.33 [1.26] years), participated in the study. Intraocular pressure increased significantly in both treatment groups compared with the preoperative values (P<.001). The mean (SD) peak intraocular pressure was significantly higher in the rimexolone-treated group, 19.7 (6.1) vs 17.6 (4.6) mm Hg (P<.001). Similarly, the mean (SD) net increase in intraocular pressure (P<.001), was also higher in the rimexolone-treated eyes, 5.9 (4.4) vs 3.9 (4.1) mm Hg (P<.001). In addition, a greater percentage of the rimexolone-treated patients had no conjunctival erythema on days 13 (11.1% vs 0.0%) and 20 (88.9% vs 55.6%) (P =.03). CONCLUSIONS: Rimexolone seems to be a more effective anti-inflammatory agent than fluorometholone. However, unlike adults, the ocular-hypertensive effect in children treated with rimexolone was higher. It would be desirable to monitor the intraocular pressure regularly when rimexolone therapy is used in children.

Topical corticosteroids of limited potency promote adenovirus replication in the Ad5/NZW rabbit ocular model.

PURPOSE: To determine the effect of topical therapy with several corticosteroids with limited potency on viral clearance in the adenovirus type 5 (Ad5) rabbit ocular model. METHODS: Sixty rabbits were inoculated in both eyes with Ad5. On the first day, the rabbits were equally divided into four topical treatment groups: 0.12% prednisolone acetate (PA), 0.1% fluorometholone (FM), 1% rimexolone (RMX), and control. Treatment was administered four times daily, in both eyes, for 3 days. All eyes were cultured for virus on days 0, 1, 3, 4, 5, 7, 9, 11, 14, 16, 18, and 21. RESULTS: Compared with the control group, treatment with PA, FM, and RMX significantly increased the number of Ad5 positive eye cultures from days 7-21. Fluorometholone and RMX prolonged the duration of Ad5 shedding, and FM increased the mean combined Ad5 titer from days 1-5 and 7-21. CONCLUSIONS: Treatment of an experimental ocular adenovirus infection with PA, FM, and RMX for 3 days significantly enhanced adenovirus replication compared with the control group. Short-term treatment of EKC with several commercially available topical corticosteroids with limited potency may offer symptomatic relief, but may also delay viral clearance and promote office and community epidemics.

Comparison of ketorolac tromethamine 0.5% and rimexolone 1% to control inflammation after cataract extraction. Prospective randomized double-masked study.

PURPOSE: To compare the efficacy of a topical nonsteroidal anti-inflammatory agent (ketorolac tromethamine 0.5%) with that of a topical steroid (rimexolone 1%) to control inflammation after cataract surgery. SETTING: Storm Eye Institute, Department of Ophthalmology, Medical University of South Carolina, Charleston, South Carolina, USA. METHODS: Thirty-six patients were prospectively and randomly assigned to receive topical treatment with either ketorolac tromethamine 0.5% or rimexolone 1% starting the day after routine cataract extraction. Treatment was masked to both patient and investigator. Each patient had uneventful small incision phacoemulsification with placement of a foldable posterior chamber intraocular lens. Patients used 1 of the 2 antiinflammatory agents 4 times each day starting 24 hours after surgery. No antiinflammatory medications were used preoperatively, intraoperatively, or for 24 hours postoperatively. Signs and symptoms of inflammation, intraocular pressure (IOP), and Kowa cell and flare measurements were evaluated 1, 4, 7, and 30 days postoperatively. RESULTS: There was no statistically significant difference in any measurement of postoperative inflammation between the 2 groups. There was no difference in objective or subjective cell and flare measurements. In addition, there was no difference in IOP measurements between groups. CONCLUSIONS: Ketorolac tromethamine 0.5% was as effective as rimexolone 1% in reducing inflammation after cataract surgery. These results suggest that ketorolac tromethamine 0.5% is a safe and effective antiinflammatory alternative to steroids after cataract extraction.

Lipomatosis due to chronic steroid therapy.

(1) Lipomatosis (development of non encapsulated fatty masses) is a rare complication of chronic systemic steroid therapy. (2) Epidural and mediastinal lipomatosis due to steroid therapy carries a risk of symptomatic compression. (3) A dose reduction or, if possible, cessation of systemic steroid therapy almost always improves or removes the symptoms.

Pharmacological validation of a feline model of steroid-induced ocular hypertension.

OBJECTIVE: To validate pharmacologically the feline model of steroid-induced ocular hypertension. METHODS: Serial studies were conducted in domesticated adult female cats trained to accept topical ocular drug administration and pneumotonometry. To establish intraocular pressure (IOP) values for each study, measurements were performed at the same time of day for 6 consecutive days. Beginning on day 7, cats received either steroid or vehicle administered topically to both eyes three times a day for approximately 28 days. The IOP measurements were performed daily. RESULTS: After 5 to 7 days of treatment with 0.1% dexamethasone or 1.0% prednisolone acetate, IOP began to increase, reaching peak values within 2 weeks. These values were sustained throughout dosing but declined rapidly to baseline upon cessation of treatment. Maximum IOPs for the dexamethasone- and prednisolone-treated groups averaged 4.5 +/- 0.3 mm Hg (n = 12) greater than the mean IOP value obtained in vehicle-treated cats. Cats treated with 0.25% fluorometholone, 1.0% loteprednol etabonate, and 1.0% rimexolone exhibited increases of 0.6, 1.2, and 1.7 mm Hg, respectively. These values were significantly lower than those observed following treatment with dexamethasone or prednisolone. CONCLUSIONS: The ocular hypertensive effects of selected anti-inflammatory topical ocular steroids in this model are consistent with clinical findings. CLINICAL RELEVANCE: This feline model is a useful tool for assessing the potential IOP liability of novel anti-inflammatory steroids.

Pharmacokinetics, protein binding and metabolic profile of 3H-icometasone enbutate following intravenous, oral and intratracheal administrations to Sprague-Dawley rats.

Absorption, distribution and excretion of 3H-icometasone enbutate (9 alpha-chloro-11 beta,17 alpha,21-trihydroxy-16 alpha-methylpregna-1,4-diene-3,20-dione, 17-butyrate, 21-acetate, CAS 103466-73-5 CL09) were studied in male and female Sprague-Dawley rats after a single dose administration by intravenous (1 mg/kg), oral and intratracheal (2 mg/kg) routes. The metabolic profile after the different routes and protein binding were also determined. Independent of the route, the radioactivity was mainly excreted in faeces. Less than 10% of the dose were excreted in urine. The majority of the administered doses was recovered within 24 h postdose, and the total recovery of the doses administered was obtained. After oral and intravenous administration to bile-duct cannulated rats, most of the radioactivity was excreted in the bile (80% of the administered dose) and some radioactivity was found in the faeces. It can thus be concluded that some intestinal secretion occurred. After oral administration, mean maximum blood concentrations were obtained about 0.75 h postdose. For the intratracheal route, the radioactive dose administered was too low to determine precise blood pharmacokinetic parameters. However, the distribution study results allowed us to conclude that the drug was absorbed first from the lungs and then from the gastrointestinal tract. Immediately after the intravenous injection, the liver, the kidneys, the small intestine and its contents and the carcass presented the highest levels of radioactivity. 168 h postdose, low radioactivity was still measurable in these organs. In other tissues, the radioactivity decreased reaching the limit of quantification 72 h postdose. After oral administration, the maximum concentrations were observed 1 h after administration in the liver, the small intestine and its contents. Then the radioactivity decreased in most of the tissues but a slight increase at 72 and/or 120 h postdose was noted in large intestine contents, carcass, lungs, eyes. After intratracheal administration, the maximum radioactivity was observed in lungs and trachea. A few minutes later the radioactivity reached the gastrointestinal tract. The protein binding study showed a saturable binding in rat and human plasma without notable differences between the two species. The binding on human serum albumin was shown to be non saturable with a total binding capacity of 7.48 +/- 1.83 mumol/l, suggesting that other proteins were involved in CL09 binding. This binding was demonstrated to be reversible. CL09 was extensively metabolized since no unchanged CL09 was recovered in bile or urine and at least nine metabolites have been detected. The profiles seemed to be different according to the route of administration.

The effects of Rimexolone 1% in postoperative inflammation after cataract extraction. A double-masked placebo-controlled study.

AIM: A multicentre, randomized, placebo-controlled double-masked study was conducted to assess the efficacy and safety of Rimexolone 1% eye drops in reducing inflammation after cataract surgery and intra-ocular lens implantation. METHODS: Rimexolone 1% (124 patients) or placebo (58 patients) was given, four times a day for 14 days starting 22-34 hours after surgery. All patients also received tobramycin 0.3% four times a day for 7 days. The clinical signs of ocular inflammation were recorded on days 1, 3, 8, 15 and 17 or 18. RESULTS: Rimexolone 1% markedly decreased the mean inflammation severity scores, and the sum of clinical assessments of cells and flare in the anterior chamber compared with placebo at each assessment. In addition, the percentage of patients with no anterior chamber inflammation was significantly higher with Rimexolone 1% than with the placebo at each assessment. All these results were statistically significant. Intra-ocular pressure did not rise after treatment with Rimexolone 1%. CONCLUSIONS: The results suggest that Rimexolone 1% ophthalmic solution is an effective and safe steroidal anti-inflammatory agent for topical use following cataract surgery and intra-ocular lens implantation.

Control of ocular inflammation after cataract extraction with rimexolone 1% ophthalmic suspension.

PURPOSE: To assess the efficacy and safety of rimexolone 1% ophthalmic suspension in controlling intraocular inflammation after cataract extraction. SETTING: Twelve independent investigational centers in the United States METHODS: This study comprised 197 patients who had cataract extraction. Postoperatively, patients were randomized to a 2 week regimen of rimexolone 1% ophthalmic suspension or a placebo. Efficacy was analyzed by monitoring total anterior chamber cells and flare, other parameters of inflammation, and treatment failures. Safety was evaluated by monitoring treatment-related adverse events and intraocular pressure (IOP). RESULTS: Rimexolone 1% was clinically and statistically more effective in suppressing cell and flare than the placebo (P < .02). The overall discontinuation rate for treatment-related adverse events was 5.3% in the rimexolone group and 22.2% in the placebo group. There were no between-group differences in IOP. CONCLUSION: Rimexolone 1% ophthalmic suspension was safe and significantly more effective than a placebo in controlling intraocular inflammation after cataract extraction when used four times daily and continued for 2 weeks.

Calcium-lowering action of glucocorticoids in adrenalectomized-parathyroidectomized rats. Specificity and relative potency of natural and synthetic glucocorticoids.

The specificity and potency of glucocorticoids to lower serum calcium (Ca) in rats after parathyroidectomy (PTX) and adrenalectomy (ADX) were examined. Rats fasted overnight were given sc injections of various steroids immediately after the operations. The fall in serum calcium 5 h after PTX-ADX in rats given hypocalcemic doses of corticosterone was compared to that after injection of a test steroid. At high doses, progesterone, estradiol, testosterone, and aldosterone were inactive, whereas glucocorticoids were consistently hypocalcemic. These results indicate that the Ca-lowering effect is specific for steroids with glucocorticoid activity. Potency estimates were made by comparing the dose-response of natural and synthetic glucocorticoids to that of corticosterone, the major glucocorticoid in rats. The mean potency of hydrocortisone was 8.2 times that of corticosterone. Prednisolone was about 9.6, triamcinolone 33, betamethasone 109, and dexamethasone 301 times as potent as corticosterone. Thus, the use of the calcium-lowering action as a bioassay has provides a specific and rapid in vivo method to compare potencies of glucocorticoids consistent with those obtained by anti-inflammatory and glycogen deposition assays. The importance of this interesting calcitonin-like action of glucocorticoids in normal physiology of calcium metabolism is not yet established.