Advances in Corticosteroid Therapy for Ocular Inflammation: Loteprednol Etabonate
نویسندگان
چکیده
Topical corticosteroids are effective in reducing anterior segment inflammation but are associated with adverse drug reactions (ADRs) including elevation of intraocular pressure (IOP) and cataract formation. Retrometabolic drug design has advanced the development of new corticosteroids with improved therapeutic indices. Engineered from prednisolone, loteprednol etabonate (LE) has a 17α-chloromethyl ester, in lieu of a ketone group, and a 17β-etabonate group. LE is highly lipophilic and binds with high affinity to the glucocorticoid receptor; any unbound LE is metabolized to inactive metabolites. LE has been studied in several anterior segment inflammatory conditions (giant papillary conjunctivitis, allergic conjunctivitis, anterior uveitis, and keratoconjunctivitis sicca), and in postoperative ocular inflammation and pain. Combined with tobramycin, it is effective in blepharokeratoconjunctivitis. Elevations in IOP are infrequent with LE, and the absence of a C-20 ketone precludes formation of Schiff base intermediates with lens proteins, a common first step implicated in cataract formation with ketone steroids.
منابع مشابه
A convenient synthesis of the side chain of loteprednol etabonate--an ocular soft corticosteroid from 20-oxopregnanes using metal-mediated halogenation as a key reaction.
A facile synthesis of the side chain of loteprednol etabonate, namely, chloromethyl-17α-[(ethoxycarbonyl))oxy]-11β-hydro of loteprednol etabonate, viz., chloromethyl-17α-[(ethoxycarbonyl))oxy]-11xy-3-oxoandrosta-1,4-diene-17β-carboxylate--an ocular soft corticosteroid, has been described starting from a 20-oxopregnane, namely, 3β-acetoxy-pregn-5(6),16(17)-diene-20-one (16-dehydropregnenolone ac...
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PURPOSE To review comprehensively the available peer-reviewed published articles in the literature on loteprednol suspension, gel, and ointment in the treatment of ocular inflammation and pain following ocular surgery. METHODS We conducted a PubMed literature search review of all published articles on keywords associated with loteprednol etabonate and ocular surgery. RESULTS A total of 59 p...
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The eye has protective barriers (ie, the conjunctival and corneal membranes) and defense mechanisms (ie, reflex tearing, blinking, lacrimal drainage) which present challenges to topical drug delivery. Topical ocular corticosteroids are commonly used in the treatment of anterior segment diseases and inflammation associated with ocular surgery, and manufacturers continually strive to improve thei...
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The efficacy of topical corticosteroids as ocular anti-inflammatory agents following cataract surgery is well-documented. They also help to prevent a number of complications associated with post-operative ocular inflammation, including corneal edema and cystoid macular edema. However, topical corticosteroids are associated with side effects, such as increased intraocular pressure (IOP). Indeed,...
متن کاملOcular Pharmacokinetics of a Novel Loteprednol Etabonate 0.4% Ophthalmic Formulation
INTRODUCTION Topical ophthalmic formulations of corticosteroids are commonly used to treat a variety of ocular diseases and conditions that have an inflammatory component. The purpose of this study was to evaluate the effect of the mucus-penetrating particle (MPP) technology on the pharmacokinetic profile of loteprednol etabonate in the ocular tissues of rabbits. METHODS Forty-eight New Zeala...
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ورودعنوان ژورنال:
دوره 2012 شماره
صفحات -
تاریخ انتشار 2012