Oxymetazoline may be a good treatment for 2 years

The dermatology news sheet Dermatology Times has published an item to their web site about the emerging use of oxymetazoline to treat the redness and flushing associated with rosacea. This article draws from the Nov. 2007 paper that introduced us to the possibility of treating rosacea with oxymetazoline.

We also know from the Feb. 2008 meeting of the AAD that oxymetazoline is effective for up to 6 hours after application, and that no negative side effects have been seen after 3 months usage. Further comments here in the DT article extends the apparent `durable’ treatment period to 2 years. Note that this successful long term avoidance of rebound whilst using oxymetazoline refers to just one patient.

Dr. Shanler notes that loss of effectiveness and rebound dilation is a problem associated with the use of intranasal use of oxymetazoline.

Oxymetazoline is classified as a alpha-1 Adregenic Receptor Agonist, whereas COL-118/Sansrosa is a alpha-2 Adregenic Receptor Agonist. According to this DT article oxymetazoline is “also partially selective for the alpha 2a receptor.”

The paper’s authors are both corporate officers of Aspect Pharmaceuticals, who are now planning more formal studies to evaluate rosacea friendly formulations of oxymetazoline and other alpha-1 adrenergic agonists to treat the redness and flushing of rosacea.

From: Taking the red out of rosacea: Topical alpha-1-adrenergic receptor agonist shows promise

Limited experience in a small number of patients indicates that the erythema and flushing associated with rosacea may be safely and successfully treated with topical application of a selective alpha 1-adrenergic receptor agonist, such as oxymetazoline, researchers say.

“The results achieved with topical oxymetazoline are exciting, but very early, and they need to be confirmed through more rigorous studies,” Dr. Shanler tells Dermatology Times.

Patient responses to topical oxymetazoline were based on direct clinical assessment and review of high-resolution digital photographs taken pretreatment at one, two to three and 24 hours post application, and then again after longer-term treatment. The evaluations showed topical oxymetazoline had a rapid effect in reducing erythema.

With continued treatment, which extended up to two years in one patient, the responses remained durable, with no evidence of tachyphylaxis, rebound or adverse events.

“Loss of efficacy due to receptor desensitization and rebound vasodilation is a problem associated with use of intranasal oxymetazoline and other imidazoline- and amine-class nasal decongestants.

“There is some laboratory evidence that the potential for receptor desensitization varies depending on the agonist’s selectivity for different alpha-adrenoreceptor subtypes and its duration of action. This may be a consideration in the development of a dermatologic medication that will provide optimal efficacy with minimal risks,” Dr. Shanler says.

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

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6 Reader Comments

  1. This is encouraging news – don’t you all think ? that it looks like oxymetazoline may be useable and work without problems for as long as 2 years.

  2. Ben says:

    My guess is with these alpha 1 and 2 receptor agonists… although I am not sure of this… that they will be effective for a time (say a year or two) and then you will have to go off them for a while and go back on… basically in the same way you do with doxy. Basically in the same way you do with many meds.

  3. Hi Ben, sounds like a good guess to me. I suspect that we don’t really know what is happening at the micro level, and whether the benefits are sustainable. I had a fear that these topicals are too good to be true, that they will blow up after regular and prolonged use. That fear might not be founded – lets all hope so.

  4. Onw way to reduce or prevent receptor desensitization, see – http://www.bio-balance.com/ijp.pdf

  5. Not sure how long it will be kept up for, but you can download a full copy of the PDF of the research paper that started this interest in Oxymetazoline here ;

    Successful Treatment of the Erythema and Flushing
    of Rosacea Using a Topically Applied Selective
    α 1-Adrenergic Receptor Agonist, Oxymetazoline


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