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Thread: More news about Brimonidine

  1. #1
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    Default More news about Brimonidine

    Check this out --

    http://www.skinandallergynews.com/ne...97ef83fdb.html


    Eye and Nasal Drugs Tame Rosacea

    By: Bruce Jancin, Skin & Allergy News Digital Network

    04/07/10

    |
    WAIKOLOA, Hawaii - Glaucoma eye drops and a nasal decongestant spray are two seemingly unlikely yet quite effective off-label therapies for the redness and flushing of rosacea.

    "For patients who are having a big problem with flushing [or] blushing, brimonidine [Alphagan] is a great drug. I use it routinely in my office," Dr. Guy F. Webster said at the annual Hawaii Dermatology Seminar sponsored by the Skin Disease Education Foundation.




    Dr. Guy F. Webster

    "I prescribe the 0.15% concentration and tell patients to put a couple of drops on their fingers, rub it onto their cheeks, see how long the effects last, and then use it accordingly. Typically, you can get through a workday with one application," according to Dr. Webster of Jefferson Medical College, Philadelphia.

    Brimonidine, whose approved indication is glaucoma, is an alpha-2-adrenergic receptor agonist and thus a vasoconstrictor. So is oxymetazoline, an over-the-counter nasal decongestant sometimes sold as Afrin and other brand names. Dr. Webster has his rosacea patients spray it on their cheeks.

    "The redness will go away for a few hours. It's a pretty darn good drug and seemingly safe," he commented.

    About 15 years ago, there were reports of a big rebound effect following chronic use of nasal decongestants for their indicated purpose. That doesn't seem to be a problem when oxymetazoline is applied to the skin, in Dr. Webster's experience, and as also borne out in a published detailed case report by another dermatologist (Arch. Dermatol. 2007;143:1369-71).

    Dr. Webster said he likes brimonidine because it's his clinical impression that the drug not only relieves the flushing and redness of rosacea, but it also improves the fixed telangiectasias that are often present. Oxymetazoline does not have that effect.

    Both drugs are now in formal clinical trials aimed at winning an indication for treatment of flushing/blushing in rosacea patients. There are no drugs approved for that purpose at present.

    Oral flush blockers that are used off-label include clonidine, which curbs menopause- and carcinoid-related flushing but "is a waste of time in the average rosacea patient," according to Dr. Webster, because it can't touch flushing induced by heat, red wine, chocolate, or other triggers. Aspirin inhibits the flushing associated with nicotinic acid therapy for dyslipidemia but is "otherwise useless" for the flushing/blushing of rosacea, he continued.

    Rosacea has four major diverse manifestations: the papulopustular, phymatous, vascular, and ocular forms. Dr. Webster commented that he is often asked if there will ever be one drug that effectively treats all these seemingly distinct subtypes. Perhaps, he said. But if it's going to happen, then it will likely be a drug that interrupts the neurologic trigger for flushing and blushing, which may be the common underlying trigger.

    "The one thing we can say with absolute certainty is that there is something neurologically weird about rosacea patients," he observed.

    Dr. Webster disclosed that he serves as a consultant to or has other financial relationships with a number of pharmaceutical companies, including Allergan Inc., which markets brimonidine.

    SDEF and this news organization are owned by Elsevier.

  2. #2
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    Default Brimonidine

    My V Beam doctor has just prescribed Brimonidine for me.

    To clarify, Brimonidine is NOT Afrin.

    Afrin is Oxymetazoline, while Brimonidine is Brimonidine Tartrate.

    Afrin apparently has other ingredients, some of which may be irritating to the skin.

    My wonderful and caring V Beam doctor may be wrong, but he thinks these two drugs are substantially different, and that the Brimonidine has much less chance of irritating things.

    I've actually had the prescription for a month. I've used it on the occasional catastrophic flush that unfortunately some of us know.

    I'm talking about the dark purple flushes that take four hours to move across my face like a slow wave and rocket my pain to almost unendurable levels.

    It reels those flushes in within half an hour, quite a change from the evening of pain I'm used to.

    But Dr Masters wants me to try it as a pophylactic. One drop in the morning on the wretched right cheek.

    I'm going to try it and promise to keep you posted.

    Am cautiously optimistic here.

  3. #3
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    By the way, Brimonidine is an eyedrop solution that's a prescription.

    I get the .2%, for those of you who want to ask your doctor for it.

    Here's how I apply it.

    I cup my left hand. Add a pea sized amount of Finacea to the hand.

    Add one drop of cold water to the Finacea.

    Add ONE DROP, NO MORE, this stuff is powerful, to the Finacea water mix.

    Stir it around with my finger and gently paint it across the wretched right cheek.

    My rosacea is almost totally centered on my right cheek, apparently an unfortunate byproduct of forty years of untreated sinus infections (remember the body brings blood to infections and over vascularized the area in response to the chronic infections).

    My rosacea is also worsened by peri menopause and only blunted by Clonidine 50mcg 3xday; Remeron 30mg nightly; Bisoprolol (Zebeta, Beta Blocker, 5mg nightly) and a low carb diet and very strong air conditioning.

    So far, the Brimonidine blanches out the wretched, chronically flushing diseased cheek, and keeps it pale for about 30 hours. One drop does that. It's amazing.

    No dermatological irritation.

    No rebound flushing when I test it by stopping.

    I'm hoping this may be the help I need to get through menopause until my body quits inflicting these horrendous hormonal storms of change upon my damaged face.

    Happy to answer questions and keep you posted.

    This is the most help I've gotten since five incredibly vicious purpuric V beams.

    Of which I will apparently need many more.

    Cheers to all of you.

    WC

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    Default Brimonidine, more

    Forgot to add that I asked Dr Masters about rebound flushing from Brimonidine.

    He said that nasal sprays cause rebound flushing when used in the nose.

    But his research indicates that Brimonidine, (a glaucoma drug, NOT a nasal spray), does NOT cause rebound flushing when used off label, topically, on a rosacea face.

    And that's been my experience, too -- no rebound effect.

    My rosacea breaks through everything I throw at it. If this stuff works well, it'll be a godsend and I will highly recommend it.

  5. #5
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    Hey WC,
    That is wonderful news! I tried it a few times but perhaps I didn't give it enough of a chance. I was afraid of a rebound effect which I thought I had experienced when I tried the drop but your success has given me new hope.

    What is the rationale for using it with Finacea?

    Best wishes for continued success!!

    Melissa

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    I use it with Finacea because the Finacea is good for my skin and I need to use it anyway, and also because the Brimonidine is so strong that I need a way to dilute it.

    Diluting it in the Finacea seems to be incredibly effective.

    I'm amazed at how much this lessens the relentless flushing I've been struggling with for so long.

    Be sure you use Brimonidine, not Afrin, if you try it. You have to get a prescription for it and it's off label since you're putting a glaucoma drug intended for eyes onto your facial skin.

    Cautiously but wildly optimistic here.

  7. #7
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    Default Brimonidine really helping me

    As many of you know, I have severe, aggressive, debilitating vascular rosacea.

    My wonderful V Beam doc, Mike Masters in Clyde NC, recently prescribed Brimonidine eye drops to use on my facial skin for my persistent flushing.

    The results have been better than I dared hope.

    I mix a drop of the Brimonidine with a bit of Finacea or moisturizer and put that on my face.

    It holds in the flushing with no irritation and no rebound flushing. I'm hard to impress and my rosacea breaks through everything I throw at it, but this stuff impresses me.

    It's a prescription eyedrop that you have to get from your doctor. I get the .2% solution and use one drop on each half of my face.

    Here's another article that mentions it. Highly recommended.

    http://healthy-aging.advanceweb.com/...a-Dilemma.aspx
    ************************************
    The Rosacea Dilemma

    Physicians are still not sure what causes rosacea, requiring them to tailor treatment plans to each symptom.

    Arisa Ortiz, MD
    Vol. 5 • Issue 2 • Page 13
    The face is the first thing a person sees, casting impressions within seconds.

    This is why rosacea, a chronic skin disorder primarily of the central face, can be so devastating for patients. Characterized by clinical signs of flushing, erythema, telangiectasia, papules, pustules, ocular lesions, and, in severe cases, rhinophyma, patients with rosacea often struggle with insecurities that affect their social and professional lives.

    Unfortunately, physicians are not sure what causes this condition, leaving us with empiric treatment of its signs and symptoms. However, several treatment strategies, including lifestyle changes, topical medications and systemic medication, can help control these symptoms.

    What is Rosacea?

    To understand how to treat rosacea, we must first discuss its manifestation. The condition commonly strikes fair-skinned individuals in their thirties, but Asians and African American have also been known to develop rosacea. In addition, rosacea can strike at any age in both men and women. We are not sure of the true incidence of the condition, largely because it is not fully characterized. However, one epidemiologic study in Sweden showed a prevalence of 10 percent in the population.1

    To provide guidance in treating the disease, The National Rosacea Society developed a standard classification system in 2002 to address the diversity of clinical manifestations, etiology and pathogenesis of rosacea.2The system describes the primary features of rosacea and defines four subtypes and one variant. (See Table 1.)

    Patients need to display just one of these primary features, such as flushing (defined as transient erythema), persistent redness, papules, pustules and telangiectasia. In addition, secondary features may also occur in addition or alone. Secondary features include burning or stinging, elevated red plaques, dry skin, edema, ocular manifestations, and peripheral location and phymatous changes, such as rhinophyma.

    Unfortunately, the pathogenesis of rosacea is still a mystery. Likely various etiologic factors come into play. We know, for example, that patients with rosacea often have abnormal vascular hyperactivity, as evidenced by facial flushing. Climate also seems to play a role, specifically exposure to the sun and extreme cold. For example, rosacea appears to be more prevalent in northern climates with frequent harsh climates. Some theories suggest that solar elastosis can alter connective tissue, which can reduce support to small vessels. This results in prolonged vasodilatation and secondary immune complex deposition, associated with the condition.

    Another theory of rosacea is the pathogenic role of Demodex folliculorum. Demodex is a mite that lives primarily within the sebaceous follicles of the central face. More Demodex mites have been found in rosacea patients compared to normal individuals.3However, the increase in Demodex mites may actually be a side effect of the condition rather than a cause. It could also simply be an exacerbating factor in these individuals.

    H. pylori is another microorganism that has been investigated for its possible pathogenic role. Support for this theory is considerably lacking, however. Most evidence now shows that the association is simply a coincidence of two common conditions that respond to similar therapies.

    Recent evidence has also shown abnormally high levels of cathelicidin, antimicrobial peptides known to induce skin inflammatory responses, in the facial skin of rosacea patients in forms that are different from those present in normal skin. LL-37 was one of the main antimicrobial peptides found in rosacea, but not found to be abundant in normal skin. LL-37 was shown to induce erythema and vascular dilatation in vivo in mice, which demonstrates an association between the clinical presentation of rosacea and abnormal cathelicidin expression.4Since we don't have a complete understanding of rosacea's pathogenesis, we generally tackle specific symptoms rather than eradicating the disease. Unfortunately, rosacea tends to wax and wane despite therapy. As physicians, we need to provide a multifaceted approach.

    Everyday Solutions

    One of the easiest things for patients to do is to avoid triggers. Thus, patients may have to eliminate spicy foods and caffeine from their diets. In addition, stress, extreme temperatures, hot beverages and alcohol can cause flare-ups of the disease.

    Patients should also use non-irritating, hypoallergenic, noncomedogenic creams, lotions, soaps and cosmetics to decrease the risk of irritation. I also suggest avoiding the sun and using sunscreen with an SPF of 30 or higher. Physical blockers such as titanium dioxide and zinc oxide are usually well tolerated. A sunscreen with a green tint may help improve the appearance of erythema as well.

    Topical Measures

    I often suggest topical medications to patients with mild-to-moderate cases of rosacea. These tend to have slower onset, but fewer safety concerns than oral medications. These measures can also help maintain remission.

    I commonly prescribe topical metronidazole to treat rosacea. This works to combat inflammatory lesions and the inflammation that manifests in generalized erythema. Azelaic acid appears to be as effective as metronidazole.5The mechanism of action of azelaic acid is unknown, but it has been shown to possess antimicrobial activity against P. acnes.6

    In other cases, I may suggest topical sodium sulfacetamide and sulfur preparations, but patients are often unhappy with the "rotten egg" odor associated with the products. Thus, I usually reserve this for patients who do not tolerate other therapies or recommend it as an adjunct for more severe disease.

    In patients with inflammatory papules, benzoyl peroxide can also be useful, but many patients with rosacea find it irritating. An alternative would be topical antibiotics, such as erythromycin or clindamycin, which have also been shown to decrease the inflammation associated with rosacea.

    A newer trend on the market is topical combination products that combine benzoyl peroxide with antibiotics such as clindamycin or erythromycin. These products allow for better compliance and ease of use. Finally, tretinoin has also been used in rosacea with some success.

    Some over-the-counter products may also give relief. Recent clinical trials conducted at the University of California, Irvine have studied the effectiveness of a new moisturizing lotion, Pyratine XR™ (0.125%) for improving the signs and symptoms of rosacea.

    Pyratine-6 (Furfuryl tetrahydropyranladenine) is a plant cytokinin that has growth modulatory, anti-oxidative and anti-senescent effects on human skin cells.7Studies show this product also improves the signs and symptoms of rosacea-as well as benefit photodamaged skin.8In one study, more than 50 percent of subjects with rosacea showed improvement as early as four weeks. After 12 weeks of treatment, 80 percent of the subjects showed overall clinical improvement in rosacea. There was a 30 percent decrease in total lesion count by week four and a 40 percent decrease after 8 to 12 weeks of treatment. Erythema was reduced by 17 percent in 12 weeks, and telangiectasia by 12 percent. More recent findings, presented at the Annual Meeting of the American Academy of Dermatology this year, also showed progressive improvement in erythema, lesion counts and telangiectases without any adverse effects with continued use.

    Some other products currently under development for the treatment of erythema associated with rosacea include Sansrosa™ and oxymetazoline. The active ingredient in Sansrosa™ is brimonidine, an alpha2-adrenergic receptor agonist, which works as a vasoconstrictor. Therefore, brimonidine can be toxic when there are high levels of systemic absorption. A phase II clinical trial tested the bioavailability of brimonidine when applied topically to diseased rosacea skin. The results of this trial have not yet been released. However, a patent application for brominidine appears to have been filed.

    Oxymetazoline is an alpha1-adrenergic receptor agonist that has had some promising results in improving the erythema in rosacea. However, researchers have yet to perform large clinical trials.

    Systemic Therapies

    Systemic therapies are effective for rosacea because they have a more rapid onset. However, I reserve this treatment for more severe cases, including inflammatory lesions, ocular rosacea, flushing or recalcitrant cases. These medications carry potential side effects, including gastrointestinal upset and candida. We also have to use caution prescribing these drugs to women who are pregnant or who may be getting pregnant.

    Oral antimicrobials help to control rosacea through their anti-inflammatory properties rather than their antibacterial effects. Higher doses are initially used to get the disease under control and then tapered down to a maintenance dose to minimize these side effects. The optimal goal is to completely transition patients onto topical treatments since unnecessary high doses and/or extended courses of antibiotic can cause antibiotic resistance.

    Newer formulations of antibiotics work to solve this problem. These drugs are low dose and extended release. Because they are sub-antimicrobial, they decrease the chance of antibiotic resistance, but they still provide the anti-inflammatory properties. Commonly used antibiotics for inflammatory lesions or ocular rosacea include erythromycin, azithromycin, tetracylcines, minocycline, doxycycline and metronidazole. Oral isotretinoin is reserved for severe or recalcitrant forms of rosacea associated with inflammatory lesions. The duration of its effect can be variable. Medications to reduce flushing such as beta-blockers, clonidine, naloxone and SSRIs can be useful, but they all have side effects that must be weighed.

    Vascular laser therapy is considered the mainstay of treatment for telangiectasia and rhinophyma and may also be effective for reducing erythema. For example, pulsed dye lasers target oxyhemaglobin in telangiectasias, which are mostly unresponsive to topical and oral therapies. Pulsed dye lasers cause vessel reduction with minimal damage to surrounding tissues. Another laser modality, intense pulsed light (IPL), targets hemoglobin, making it effective in treating telangectasia. However, with the natural progression of aging, new vessels develop.

    Nonablative lasers may also be effective in rosacea by improving the epidermal barrier and remodeling of dermal connective tissue. In addition, another common component of the condition, rhinophyma, can be resurfaced by mechanical dermabrasion, carbon dioxide laser, electrocautery, paring with a scalpel, or excision with skin grafting.

    As stated previously, current therapy aims at treating individual elements of rosacea. This usually means that more than one therapy is generally used simultaneously. Therapies should be tailored to the particular symptoms of the patient and their own preferences.

    ****************

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    Wow, WrinkledClue - this sounds fabulous. Do you use this once a day (ie. one drop on each cheek)? How many days have you used Brimonidine?

    Please let us know how things continue to go.

    Thank you.
    Yvette

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    Hello Yvette,

    Every morning I mix one drop of the Brimonidine with a large dollop of Finacea and a bit of of cold water.

    I mix this with my finger, and paint half my face with it.

    Then I do the same thing to the other side.

    The results are really spectacular.

    Like many of us, I have a baseline of redness even when I'm not flushing, from years of damage.

    The Brimonidine makes it so that the skin on my face becomes the same color as the skin on my neck. And it stays that way, all day and all night.

    And so far there's no rebound vasodilation if I skip the Brimonidine the next day.

    No skin irritation either.

    I've struggled with severe progressive rosacea for years now, and I can hardly believe the success I'm having with this.

    Many of us here know the frustration of not being able to join your friends in a warm restaurant, or walk with your honey on a warm summer night, or even go into some stores that are not adequately air conditioned, lest you suffer a painful flush.

    This seems to have tremendous potential to raise the temperatures I can comfortably stand before I flush.

  10. #10
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    Default Important caution about wonderful Brimonidine

    This prescription eyedrop for glaucoma called Brimonidine is really helping my wretched face.

    But I wanted to caution you NOT to put it directly on your face. It's too strong. If you put it directly on your face, you'll get a wierd looking blanched-out circle that will get white within an hour or two and stay white for about 24 - 30 hours.

    Instead, you have to dilute the Brimonidine with a cream or moisturizer.

    I put a dollop of Finacea in one palm, add a drop of water, and then add ONE DROP of Brimonidine to it. Stir with a finger and use that to paint half my face. Repeat on the other half of my face.

    Results after about one week of use, so far, are simply spectacular. And I'm hard to impress, with severe, progressive, debilitating flushes.

    Those of you who've seen my thread In Praise Of Purpuric V Beam can see photos of how bad my flushes are.

    The big news here is really that my V Beam doctor feels it's safe to use Brimonidine as a preventative. He's seen my flushes, he's appalled by them, he knows they're damaging my skin, and he wants me to use the Brimonidine daily to stop those flushes from happening in the first place.

    So far, it's working.

    Highly recommended!

    Happy to answer questions!

    WC

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