Site-active steroid provides symptomatic relief for patients with dry eye disease

May 15, 2005

Miami—Anti-inflammatory treatment using loteprednol etabonate suspension 0.2% (Alrex, Bausch & Lomb) appears to offer a safe and useful option for symptomatic relief in patients with dry eye, according to Roberto Beraja, MD.

Miami-Anti-inflammatory treatment using loteprednol etabonate suspension 0.2% (Alrex, Bausch & Lomb) appears to offer a safe and useful option for symptomatic relief in patients with dry eye, according to Roberto Beraja, MD.

Dr. Beraja, a private practitioner in Miami, says he particularly likes to prescribe the topical corticosteroid in older patients who complain of dry eye and are not achieving adequate relief from artificial tears alone. Patients are instructed to use loteprednol etabonate 0.2% up to four times a day as needed.

"I like to use this agent as a first-line treatment before prescribing cyclosporine because I find it is helpful administered on a prn [pro rata nata, i.e., as needed] basis. Typically, patients will use the loteprednol etabonate 0.2% for several days if they are experiencing a flare of symptoms, but once they are more comfortable, they are able to resume treatment with artificial tears alone," Dr. Beraja said.

In addition, patients are examined for other treatable conditions that may be contributing to their dry eye problem, such as blepharitis.

"In those situations, I also address the underlying external disease, but I prescribe the loteprednol etabonate to gain acute symptomatic control and tell patients they may re-initiate the loteprednol as needed if their symptoms suddenly worsen," Dr. Beraja said.

He is very comfortable letting patients use loteprednol etabonate 0.2% at their own discretion because of its excellent safety profile. Although loteprednol etabonate is a structural analogue of prednisolone, unlike its parent molecule and other corticosteroids that are used in the eye, loteprednol features an ester group instead of a ketone at the C20 molecular position. As a result of that modification, loteprednol etabonate is a "site-active" steroid.

After it is placed into the eye, loteprednol etabonate exerts its anti-inflammatory effect, but then it is rapidly metabolized by local esterases into inactive metabolites.

"Some increases in IOP have been reported in clinical trials of loteprednol etabonate," Dr. Beraja said. "However, the rate of clinically significant increases in IOP was only 1% in patients treated with loteprednol etabonate 0.2%, which was identical to that associated with placebo, and I have not yet encountered any patients whose IOP increased in association with using this product.

"As a precaution, however, I do not prescribe loteprednol etabonate 0.2% to treat dry eye in any patients with a known diagnosis of glaucoma," Dr. Beraja said.