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Advances in Corticosteroid Therapy for Ocular Inflammation: Loteprednol Etabonate

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...

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Detalles Bibliográficos
Autores principales: Comstock, Timothy L., DeCory, Heleen H.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Hindawi Publishing Corporation 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3321285/
https://www.ncbi.nlm.nih.gov/pubmed/22536546
http://dx.doi.org/10.1155/2012/789623
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author Comstock, Timothy L.
DeCory, Heleen H.
author_facet Comstock, Timothy L.
DeCory, Heleen H.
author_sort Comstock, Timothy L.
collection PubMed
description 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.
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spelling pubmed-33212852012-04-25 Advances in Corticosteroid Therapy for Ocular Inflammation: Loteprednol Etabonate Comstock, Timothy L. DeCory, Heleen H. Int J Inflam Review Article 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. Hindawi Publishing Corporation 2012 2012-03-28 /pmc/articles/PMC3321285/ /pubmed/22536546 http://dx.doi.org/10.1155/2012/789623 Text en Copyright © 2012 T. L. Comstock and H. H. DeCory. https://creativecommons.org/licenses/by/3.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Review Article
Comstock, Timothy L.
DeCory, Heleen H.
Advances in Corticosteroid Therapy for Ocular Inflammation: Loteprednol Etabonate
title Advances in Corticosteroid Therapy for Ocular Inflammation: Loteprednol Etabonate
title_full Advances in Corticosteroid Therapy for Ocular Inflammation: Loteprednol Etabonate
title_fullStr Advances in Corticosteroid Therapy for Ocular Inflammation: Loteprednol Etabonate
title_full_unstemmed Advances in Corticosteroid Therapy for Ocular Inflammation: Loteprednol Etabonate
title_short Advances in Corticosteroid Therapy for Ocular Inflammation: Loteprednol Etabonate
title_sort advances in corticosteroid therapy for ocular inflammation: loteprednol etabonate
topic Review Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3321285/
https://www.ncbi.nlm.nih.gov/pubmed/22536546
http://dx.doi.org/10.1155/2012/789623
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