PURPOSE OF REVIEW: Corticosteroids are an effective short-term treatment option for seasonal allergic conjunctivitis (SAC). Their use has been limited due to their side effects and has led to the development of modified 'soft', 'smart' ophthalmic corticosteroid formulations that retain their anti-inflammatory mechanism of action with an improved safety profile. RECENT FINDINGS: Similar to the development of the prodrug concept for the nose and lung that led to the development of ciclesonide, a chloromethyl-ester group substitution at the carbon-20 (C-20) position of the traditional corticosteroid has led to the development of a family of potential ophthalmic corticosteroids including loteprednol etabonate that has demonstrated similar efficacy to the C-20 ketone corticosteroids in the treatment of the signs and symptoms of ocular allergies, but less likely to induce elevations in intraocular pressure (IOP) or the formation of cataracts. The C-20 ester corticosteroid, loteprednol etabonate has been designed to be rapidly converted to an inactive, nontoxic metabolite, thus minimizing adverse effects, and loteprednol etabonate (0.2%) is currently the only ophthalmic corticosteroid specifically developed for and approved by the Food and Drug Administration for treatment of SAC. SUMMARY: The development of modified or soft, smart corticosteroids such as loteprednol etabonate provides an avenue for expanding the treatment of the inflammation associated with signs and symptoms in patients with chronic forms or severe acute exacerbations of allergic conjunctivitis. Modified corticosteroids are an effective and well tolerated option for the short-term treatment of the inflammation and signs and symptoms associated with SAC.
PURPOSE OF REVIEW: Corticosteroids are an effective short-term treatment option for seasonal allergic conjunctivitis (SAC). Their use has been limited due to their side effects and has led to the development of modified 'soft', 'smart' ophthalmic corticosteroid formulations that retain their anti-inflammatory mechanism of action with an improved safety profile. RECENT FINDINGS: Similar to the development of the prodrug concept for the nose and lung that led to the development of ciclesonide, a chloromethyl-ester group substitution at the carbon-20 (C-20) position of the traditional corticosteroid has led to the development of a family of potential ophthalmic corticosteroids including loteprednol etabonate that has demonstrated similar efficacy to the C-20 ketone corticosteroids in the treatment of the signs and symptoms of ocular allergies, but less likely to induce elevations in intraocular pressure (IOP) or the formation of cataracts. The C-20 ester corticosteroid, loteprednol etabonate has been designed to be rapidly converted to an inactive, nontoxic metabolite, thus minimizing adverse effects, and loteprednol etabonate (0.2%) is currently the only ophthalmic corticosteroid specifically developed for and approved by the Food and Drug Administration for treatment of SAC. SUMMARY: The development of modified or soft, smart corticosteroids such as loteprednol etabonate provides an avenue for expanding the treatment of the inflammation associated with signs and symptoms in patients with chronic forms or severe acute exacerbations of allergic conjunctivitis. Modified corticosteroids are an effective and well tolerated option for the short-term treatment of the inflammation and signs and symptoms associated with SAC.
Authors: Monica Baiula; Andrea Bedini; Jacopo Baldi; Megan E Cavet; Paolo Govoni; Santi Spampinato Journal: Drug Des Devel Ther Date: 2014-06-10 Impact factor: 4.162