Loteprednol Etabonate, also known as Lotemax, is an anti-inflammatory corticosteroid eye solution. As a prescription eye drop, loteprednol etabonate, CAS number 82034-46-6, is used to treat a variety of inflammatory eye conditions. These conditions typically affect the anterior chamber of the eye and include allergic conjunctivitis, superficial punctate keratitis, acne rosacea, Iritis, herpes zoster keratitis, cyclitis and certain types of infectious conjunctivitis. A typical dose for many of the aforementioned conditions is one to two drops in the affected eye(s), administered up to four times daily. Common side effects include vision disturbances, such as blurriness, dry eye, itching, swelling of the conjunctiva, excess tear production and light sensitivity. Systemic adverse effects such as headache and rhinitis have also been noted. The first patent for Lotemax expired as recently as March 2012. LGM Pharma provides API loteprednol etabonate for R&D purposes, and provides complete support to clients throughout the research and development process.
As an ester corticosteoid, loteprednol etabonate has shown a well documented safety profile through over a decade of studies. In addition to it’s efficacy in decreasing the production of inflammatory precursor proteins, loteprednol etabonate offers increased lipiphilicity, which allows a greater cell penetration. While loteprednol etabonate is structurally similar to other corticosteroid solutions, it is unique in that the number 20 position ketone group is absent in the structure, making it a highly lipid soluble treatment. In a trial studying the safety and effectiveness of loteprednol etabonate 0.5% versus prednisolone acetate 1.0% ophthalmic suspension, loteprednol was found to have a favorable profile in regard to intraocular pressure increases. This conclusion was published in the American Journal of Ophthalmology, which revealed that the treatment of these patients with acute anterior uveitis saw less of an increase in intraocular pressure after receiving loteprednol etabonate. In opposition, patients who received prednisone acetate displayed a greater incidence of intraocular pressure increases.
Currently being explored for it’s use in treating seasonal allergies with allergic conjunctivitis, loteprednol etabonate is being marketed as such an eye drop by Bausch and Lomb, known as Alrex. The April 1, 2012 issue of Pediatric Drugs, published online, revealed results from a trial which measured both the tolerability and safety of loteprednol etabonate 0.5% and tobramycin 0.3%. These ophthalmic suspensions were tested in pediatric subjects, ages 0-6, in randomized and parallel group studies. Adverse events in the group of children who received loteprednol etabonate were deemed low, and the use of loteprednol was determined to be safe for children in short term dosing for conditions such as blepharoconjunctivitis.
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