Loteprednol etabonate ophthalmic suspension 0.5 %: efficacy and safety for postoperative anti-inflammatory use

Abstract

Topical corticosteroids are routinely used as postoperative ocular anti-inflammatory drugs; however, adverse effects such as increased intraocular pressure (IOP) are observed with their use. While older corticosteroids such as dexamethasone and prednisolone acetate offer good anti-inflammatory efficacy, clinically significant increases in IOP (≥10 mmHg) are often associated with their use. Loteprednol etabonate, a novel C-20 ester-based corticosteroid, was retrometabolically designed to offer potent anti-inflammatory efficacy but with decreased impact on IOP. After exerting its therapeutic effects on the site of action, loteprednol etabonate is rapidly converted to inactive metabolites, resulting in fewer adverse effects. Randomized controlled studies have demonstrated the clinical efficacy and safety of loteprednol etabonate ophthalmic suspension 0.5 % for the treatment of postoperative inflammation in post-cataract patients with few patients, if any, exhibiting clinically significant increases (≥10 mmHg) in IOP. Furthermore, safety studies demonstrated a minimal effect of loteprednol etabonate on IOP with long-term use or in steroid responders with a much lower propensity to increase IOP relative to prednisolone acetate or dexamethasone. The anti-inflammatory treatment effect of loteprednol etabonate appears to be similar to that of rimexolone and difluprednate with less impact on IOP compared to difluprednate, although confirmatory comparative studies are needed. The available clinical data suggest that loteprednol etabonate is an efficacious and safe corticosteroid for the treatment of postoperative inflammation.

Comparison of the Safety and Efficacy of Loteprednol Etabonate 0.5%/Tobramycin 0.3% with Dexamethasone 0.1%/Tobramycin 0.3% Following Strabismus Surgery

“…After exerting its effects, LE is rapidly metabolized by tissue esterases, limiting any potential adverse effects associated with its use. LE is reported to be highly lipophilic and has strong binding affinity to glucocorticoid receptors [4,17,18]. Compared with DM, its lipophilicity was 10 times higher and its binding affinity to a glucocorticoid receptor was 4.3 times higher [4].…”

“…LE is reported to be highly lipophilic and has strong binding affinity to glucocorticoid receptors [4,17,18]. Compared with DM, its lipophilicity was 10 times higher and its binding affinity to a glucocorticoid receptor was 4.3 times higher [4]. LE is indicated for the treatment of various ocular surface and anterior segment inflammatory conditions such as seasonal allergic conjunctivitis, blepharokeratoconjunctivitis, and uveitis [17,4].…”

“…Compared with DM, its lipophilicity was 10 times higher and its binding affinity to a glucocorticoid receptor was 4.3 times higher [4]. LE is indicated for the treatment of various ocular surface and anterior segment inflammatory conditions such as seasonal allergic conjunctivitis, blepharokeratoconjunctivitis, and uveitis [17,4]. It offers a safe and proven management of postoperative pain and inflammation after cataract surgery [6,14,17].…”

“…Loteprednol etabonate (LE), a new-generation corticosteroid, has been shown to be an effective anti-inflammatory agent with lesser side effects in anterior segment inflammatory conditions [4][5][6]. Recently, topical combination products of 0.5% LE/0.3% tobramycin (LE/T) or 0.1% DM/0.3% tobramycin (DM/T) are commonly used in the treatment of steroid-responsive ocular inflammation, and a risk of bacterial ocular infection exists [7][8][9][10][11][12][13].…”

Evaluation of Topical Cyclosporine in Preventing the Development of Corneal Haze after Photorefractive Keratectomy

“…4 However, topical steroids have their own side effects such as delayed would healing, increased risk of infection, posterior subcapsular cataracts, ocular hypertension, and glaucoma. 5,6 Because of the side effect profiles of these two common medications, refractive surgeons have long been interested in finding a medication which prevents haze and has a better safety profile than steroids or mitomycin C. A host of medications have been examined, including NSAIDS, 5,7,8 anti-VEGF and anti TNF-α compounds 9 , nicergoline and β-glucan, 10 and IL1-ra.…”