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Loteprednol etabonate, the active ingredient in Lotemax®, is a novel compound designed to be a "site-active" corticosteroid. Unlike all other ophthalmic steroids, loteprednol etabonate contains an ester group (instead of a ketone group) in its molecular structure. This structural modification allows for naturally occurring esterases in the eye to break down loteprednol into inactive metabolites after loteprednol exerts its effect. Lotemax is also highly lipid soluble, enhancing its penetration into cells and enabling it to exert anti-inflammatory activity within the eye. |
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Lotemax is designed to be active only at the site of application and to be deactivated in a predictable, single-step reaction after achieving its therapeutic role. This predictable, single-step chemical modification to an inactive metabolite2 minimizes unwanted side effects. As further proof that loteprednol is metabolized quickly:
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Results from a bioavailability study in normal volunteers established that plasma levels of loteprednol etabonate and cortienic acid etabonate, its primary inactive metabolite, were below the limit of quantification (1 ng/ml) at all sampling times.2 |
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No evidence of Hypothalamus-Pituitary-Adrenal (HPA) axis suppression were found after two weeks of therapy3 |
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Lotemax (loteprednol etabonate ophthalmic suspension 0.5%) offers the broadest range of indications of any ophthalmic steroid currently available.
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