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Abstract #19317 Published in IGR 9-3
Ester and ketone corticosteroids
Favetta JRAllergy and Clinical Immunology International 2007; 19: 16-18
Topical ketone corticosteroids (e.g., prednisolone, dexamethasone, and fluorometholone) are used to treat ocular allergies. In spite of their potent antiinflammatory effects, ketone corticosteroids cause serious adverse effects, including an increased risk of cataract formation, elevated intraocular pressure (IOP), infections, and systemic hypercorticoidism. The C-20 ketone group appears to be associated with cataract formation in ketone corticosteroids. Replacement of this C-20 group with a chloromethyl ester moiety led to the development of loteprednol etabonate, a unique ester corticosteroid and currently the only one indicated for the treatment of signs and symptoms of intermittent (seasonal) allergic conjunctivitis (IAC). Topical loteprednol etabonate may have several advantages over ketone corticosteroids. These include increased efficacy due to its high lipophilicity and ability to penetrate inflammatory cell membranes; rapid single step inactivation by local tissue esterases, minimizing the risk for ocular hypertension and optic nerve damage; and low systemic bioavailability, with a decreased potential for systemic side effects. A long-term safety study demonstrated the absence of cataracts and elevated IOP following continuous loteprednol etabonate treatment up to 12 months, suggesting loteprednol etabonate may offer a safer treatment option to topical ketone corticosteroids.
Dr. J.R. Favetta, 70 Ridge Road, North Arlington, NJ 07031, USA. johnfavetta@comcast.net
Classification:
9.4.1 Steroid-induced glaucoma (Part of: 9 Clinical forms of glaucomas > 9.4 Glaucomas associated with other ocular and systemic disorders)
