Oxymetazoline: what about rebound redness ?


One of the up and coming treatments for the redness of rosacea is the use of oxymetazoline based formulations.

Oxymetazoline is the active ingredient in decongestant products like Afrin, Sudafed OM and Vicks Sinex as well as in eye drops like Visine LR.

Recent publicity from Vicept Therapetics suggests that their product in development V-101 contains the active ingredient oxymetazoline.

A well known side effect of Visine is rebound redness, where continued use leads to the redness that you were originally treating. Extended usage of Afrin can also lead to rebound nasal congestion.

Rebound redness with eyedrop use


Oxymetazoline is a long-acting topical drug that constricts, or shrinks, blood vessels. That is how it relieves congestion in the nose. But people who use nasal decongestants for allergies, colds or sinus problems are warned to use such products for only three to five days. After that they may experience rebound congestion as the medicine wears off.

The same thing can happen in the eyes. Rebound redness occurs when the blood vessels dilate after the effects of the medicine fade. It can take several days (or sometimes longer) for this effect to gradually disappear. You may be better off with artificial tears rather than anti-red drops.

For any oxymetazoline based treatment to succeed as a treatment for a chronic condition like rosacea (i.e. rosacea isn’t a condition that goes away after just a couple of days), the promoters will need to prove that their formulations are safe for use in the medium to long term.

A 2007 paper Successful Treatment of the Erythema and Flushing of Rosacea Using a Topically Applied Selective α1-Adrenergic Receptor Agonist, Oxymetazoline attempted to answer this questions thus;

Neither of our patients exhibited either problem with the application of oxymetazoline to the skin. While the laboratory induction of receptor desensitization cannot yet be perfectly correlated with actual physiologic response, recent laboratory studies indicate that agonists that are more selective for α1D-adrenoceptors are less prone to induce receptor desensitization than are α1A- or α1B-agonists. The clinical significance of this may be an important consideration in contemplating any potential future use of these drug classes on the skin because agonists with certain receptor subtype binding profiles may retain their clinically desirable effects while minimizing their adverse effect.

(emphasis mine)

You can download a full copy of this article from the Archives of Dermatology website; Successful Treatment of the Erythema and Flushing of Rosacea Using a Topically Applied Selective α1-Adrenergic Receptor Agonist, Oxymetazoline

So we all wait to see how the trials of V-101 prove performance with extended and intermittent usage of oxymetazoline.

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About the Author

About the Author: David Pascoe started the Rosacea Support Group in October 1998. .

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