Oxymetazoline Eyedrops Has 'Modest' Effect on Droopy Eyelid

By David Douglas

October 07, 2020

NEW YORK (Reuters Health) - The recently approved oxymetazoline hydrochloride 0.1% ophthalmic solution (Upneeq) can help rectify eyelid positioning in patients with acquired blepharoptosis (ptosis), although the effect is modest, according to an analysis of data from two clinical trials.

"Treatment options for patients with acquired blepharoptosis have largely been limited to surgical intervention," Dr. Charles B. Slonim of the University of South Florida Morsani College of Medicine, in Tampa, told Reuters Health by email. "The findings of these studies provide evidence for the efficacy and safety of a non-surgical treatment."

In a paper in JAMA Ophthalmology, Dr. Slonim and colleagues note that in addition to causing an asymmetric or sleepy appearance, obstruction of the pupil by the upper eyelid can lead to superior visual field deficits and affect quality of life.

Oxymetazoline has long been used as a topical nasal decongestant. It appears to treat ptosis, also known as droopy eyelid, by stimulating alpha-adrenergic receptors in the superior tarsal muscle, causing muscle contraction and upper-eyelid lift, the authors explain.

The team analyzed data on a total of 296 patients who had participated in one of two phase-3 trials; 198 were randomized to oxymetazoline and the remaining 98 to vehicle alone. The participants self-administered a single drop per eye once daily.

On day 1 (six hours after instillation), active treatment showed a significant increase in the mean number of points seen on the Leicester Peripheral Field Test, compared to vehicle alone (5.9 vs. 1.8). At 14 days, the numbers were 7.1 and 2.4.

Marginal reflex distance 1 (MRD-1) measured at the same timepoints also showed significant improvement. At day 1, MRD-1 was 0.96 mm in the active treatment group and 0.50 mm in the vehicle group. At 14 days the values were 1.16 mm and 0.50 mm.

Treatment-emergent adverse events (TEAEs) were seen in 31% of the oxymetazoline group and 36% of the vehicle group. Most were mild, and no serious TEAE was suspected of being related to treatment; all were resolved.

There were also no clinically relevant mean shifts from baseline in vital signs, or intraocular pressure, Snellen visual acuity, pupil diameter or other examination results in either eye.

"The recent approval of Upneeq by the (U.S. Food and Drug Administration) means more therapeutic options for eye-care practitioners and for patients with acquired blepharoptosis," Dr. Slonim concluded.

Dr. Elizabeth A. Bradley of the Mayo Foundation, in Rochester, Minnesota, co-author of an accompanying editorial, told Reuters Health by email that "the main point is that the improvement in eyelid position that was seen with oxymetazoline was modest, suggesting that its role may be limited to mild cases."

However, she said, "having something to offer patients with mild ptosis, who don't want or don't qualify for surgery, could be very helpful. We still need more information to determine whether the treatment effect is sustained, and whether there are any long-term side effects such as dry eye."

The trials in the study were funded by an affiliate of Osmotica Pharmaceuticals, which markets Upneeq, and the current analysis by Osmotica. Dr. Slonim has ties to RVL Pharmaceuticals, a subsidiary of Osmotica, and his coauthors also have relationships with the company.

SOURCE: https://bit.ly/30yZbV9 and https://bit.ly/3nkxQji JAMA Ophthalmology, online October 1, 2020