The brimonidine trial: it was not what I had hoped ...(2010)

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For a long time rosacea patients waited for a product with the working title Sansrosa. A working title for the product that would later become known as Mirvaso, made by Galderma. Promises were made that it would topically shut down blood vessel dilation, and turn our rosacea faces pale. There was a real rush and excitement going through the online rosacea communities. In the meantime, around 2010, some bad flushers had already started to try an optical eye gel with brimonidine tartrate in it, as that would be more or less the type of active ingredient of Sansrosa. Here is a summary of the trial I did myself at the time. It was not what I had hoped it to be. This is a summary I wrote some time later, below is the exact stuff we discussed and wrote on the forum at the time, which is more precise. I mixed the brimonidine tartrate powder with some water (scroll down for more details on this) and applied it to my cheeks. No burning luckily from it and after about 10 minutes my skin started to feel tight. After 30 minutes it turned ghostly pale. I was elevated and excited. Whenever the effect seemed to wear off, I applied a little bit more. After some time, when I was at a party that evening, I felt the effect wearing off completely and worse, I had such bad rebound flushing and redness. There seemed no stopping, no cold pack or fan or cold air helped. Had to sit it out and it lasted about 12 hours. Way too long for me to use this substance regularly. What a shame, because initially it really seems to shut down the blood vessel dilation. But the rebound flushing seems not a good thing, especially in the long run.

2011 has overall been up and down, but a good part of the time my skin wasn't too bad, within the still severe ranges generally
I can't post the worst of the worst flushes, I wasn't in the mood to picture them, but these are some impressions of the good days and the less good days. Besides, I am still on the same medication (clonidine, propranolol, remeron, Xyzal). Left cheek (my right one) still pale from the brimonidine which was freshly applied, the other having pretty bad rebound flushing, which lasted at least 12 hours and I couldn't calm it down, whatever I tried.

Patchiness after applying the brimonidine

solution, paler spots become visible. 

 

My left cheek is evened out 

and pretty pale now. 

Left cheek (my right) is fully pale now, but the right cheek, 

where I applied the brimonidine first (waited an hour or so in between) is starting to burn and get red after 5 hrs

 On the other cheek the brimonidine also starts to wear off
after some hours. Some redness keeps breaking through and
soon there is all over redness and more flushing than before
applying the brimonidine

Next day

Update (10th december 2013)                               
I received some questions on the forum by a user named Makron about the exact sort of Brimonidine trial I did, so had to look for the exact posts I made at the time, and while I was at it, I might just as well put them here. I added some info here last night about attempting to match the 3,3 mg/ml brimonidine (free base, equaling 5 mg brimonidine tartrate) in Mirvaso back then with my own mixture, to get an similar sort of problem. Mirvaso wasn't launched yet by then however and I couldn't know the composition of Mirvaso yet. I used 2 mg/ml of brimonidine tartrate (and later some more, between 2 and 3 mg) to match the brimonidine eye gel that was tested by some rosacea patients at the time. Below are links and blog posts from 2010 to further explain this. With the remainings of my 5 gr batch of bought brimonidine tartrate, I thought at the time that I could come near the Sansrosa (working titel of current drug Mirvaso) dose during the next trial/mix, as there was still talk then that Sansrosa would consist of around 3 mg/ml of brimonidine tartrate. Instead of the 5 mg/ml brimonidine tartrate it contains now. Hence why Mirvaso now seems way too strong perhaps for some patients, and needs to be diluted according to some derms and reps. My aim back then was to match the brimonidine eye gel with 2 mg/ml of brimonidine tartrate however, as is in the forum posts from 2010, added below. (Mirvaso wasn't a point of reference back then. This poster tried to make it sound like it was for me, and that I lied about the dose and tried to match the brimonidine experience in hindsight with the current Mirvaso drug, but that is based on an already corrected inaccuracy of me in the few red summarizing sentences I added 2 nights ago here; I meant to say that our reference point while making the mix was the eye gel and erroneously summarized that we aimed for Mirvaso instead, which wasn't even out yet, and which turned out to be stronger than we then anticipated the drug to become. I did think at the time however that the second batch of home made brimonidine mix -which I didn't report on in detail like the first try as it turned out exactly the same and with even more and quicker 'rebound' (or at least very bad) flushing and redness and throbbing of the face- equalled the brimondine tartrate/base carrier ratio and in hindsight this was incorrect as Mirvaso turned out to be stronger). To be clear, I haven't used Mirvaso, as it isn't available yet here. Back in 2010 some rosacea patients mentioned they got pale skin from using a brimonidine eye gel on their face. As we said at the beginning of the mirvaso threads, these brimonidine tests are not directly comparable, as I used 2 mg/ml brimonidine tartrate and then 3 mg/ml in a water solution (not equalling the 5 mg tartrate per gram Mirvaso) and splashed a lot more than a pea size on my face. At the time, there was no Mirvaso and people were waiting for Sansrosa as it was called then for a good 5+ years already. 

Here is more of what I have written on the Rosacea Forum at the time:

18th August 2010 10:40 AM: "I tried brimonidine also several days, after dear Wrinkledclue helped me get some, and my chin was clearly paler after use. Next day some on the cheek, and I did see a lighter skin tone, but... also a rash after some time. Rough skin, so to speak and burning a bit. So my theory is, that the brimonidine is working but the preservative and alcohols that are added to the ophthalmic solution are too much for my paper thin skin. So, tried to order some pure brimonidine powder from the pharmacist, but available (sic; unavailable).... Probably because the pharmaceuticals (Falcon in this case) won't give away the active ingredients. So I googled and found some suppliers in China (..). Emailed some of them and the problem now is that they send it in a big dose, minimum of 100 g. mostly (which costs about 800 US dollars!!) and I could get 5 g. from one supplier, for 200 US dollars. Now, I am a big dumbo with those measuring quantities. What do you guys think? It seemed very little to me, 5 g, but then I saw the solution and it only has 0,2% brimonidine in it. So perhaps 5 g is quite a lot actually then? I discussed it with the pharmacist and he said that he can either put the powder in a cream or gel for me, or I can mix it myself daily with water, so we don't need a preservative. I will have to find out how much powder exactly I can use in a drop of water, don't want it to be too much... What do you guys think? These Chinese factories supply the product to the big pharmaceuticals, so I hope it is safe. What about the price? Seems very high to me, but I don't know how much we would need for daily use? And perhaps there are more people interested in this and want to join in?"

Then on 2nd September 2010 05:05 PM: "Ok, the brimonidine powder arrived! Just a small sealed see through bag with whit´ish powder in it. Did email the Chinese woman again to stress again how important it is to have proper brimonidine so I can truly give it a try and perhaps pass the company details on if it works, so I guess it´s a matter of trust now, and perhaps even white skin! A friend has a very precise measuring thing, to my surprise (for honey actually) and I have been able to measure 0,2 g. I have put it in 100 ml of bottled water, all things first sterilized in boiling water. And I have patted the solution on my chin and part of my right cheek AND make pictures of the skin, so perhaps I can detect pale skin in some time. The skin is feeling a bit tingling and numb´ish now, not really numb but it feels a little bit different then the other skin. No burning though, nothing uncomfortable. I am a little bit afraid it will do nothing and I just threw away 200 dollars... To be continued...

2nd September 2010 09:12 PM: So far so good. I put the brimonidine solution on my lower left cheek and chin and within time white patches showed. I have put more of the solution on the spaces in between and it´s still patchy, but def. very pale patches. Chin is completely pale now and left lower cheek has very clear patches. My skin seems to handle it, although it feels ´tight´ and a bit numb at the same time and can tingle. It´s weird, not painful. I am aware of the feeling of the skin, unlike other normal skin. But nothing too bad. Have to see now if the dreaded rebound flare comes. Does anyone have an idea how I can avoid the patches and just have even pale skin? Will mail Tony Chu as well about it, I know he´s interested in this and perhaps he also (like my pharmacist on the phone) has an idea about the percentage and solution. I don´t understand why it shows in patches.....To be continued..

2nd September 2010 10:39 PM: Ai ai ai, this is looking promising! I´m not easily positive when it comes to rosacea, but my cheek (I wrote left cheek, but just realized that´s on my pictures, its actually my right, detail) is PALE. Stays like that when facing a trigger (and the other one does flare up).The patchiness is still there but seems to fill up a bit and the difference is quite dramatic I think. Skin feels still a little bit tight but that´s about it. Note that my upper skin is paper thin and always irritated and dry, so I expected more troubles from it. I just can´t believe this, and am sort of waiting for the disappointment to throw me back in reality. Will see how the cheek is tomorrow morning and if still good, will put the solution on both cheeks then. Just thin from what I understood this brimonidine is the active ingredient also in the upcoming Sansrosa cream. But wouldn't it be much better for rosaceans to mix the active ingredient themselves into either water or their own cream? I am almost certain there will be some kind of alcohol or preservative in that cream. This way we have the pure active ingredient and almost no irritants to the skin. Thanks Wrincledclue for suggesting the brimonidine eye drops!!!!

3rd September 2010 10:13 AM: this morning still pale on the treated area´s, the rest moderately flushed. So far no other side effects. I called the pharmacist to ask how I can store the solution. I first disinfected the weighting scale and measuring cup in boiling water and used bottled water from a sealed bottle by the way, just to be on the safe side. He said that it can be stored in the fridge, to preserve it longer. The molecules of brimonidine are small he said and it´s very soluble to water, so he doesn´t expect crystals to be formed in the fridge. I put the solution straight on my face. I put some of the liquid in a little cup and put it on my skin with my finger, as much as needed and I also ´paint´ more on the patches that are blotchy. Not sure if this is too much though, as it´s the strength of the normal eye drop solution, but it´s been working.. I have ordered the 5 g sample here:

sales6@sinochem-nanjing.com

Miss Fairy Yang

The corporation is Sinochem Nanjing, website: http://www.sinochem-nanjing.com/

3rd September 2010 08:32 PM: Very bad rebound in right cheek. Left one is fine for some reason. The right cheek has already a red patch this morning but now it´s full blown all over the cheek, haven´t had it this bad in a long time. Not sure if it is brimonidine related, I did have some irritation from indirect sunlight earlier this week, but this is really full force flushing. Will give my skin some days to calm down again and see again.   
                                                                                            
4th September 2010 10:58 AM: Big flare on the left cheek as well this morning. Am having two red flushed cheeks again. Am sure now that it has to do with the after effect of the brimonidine, as the left cheek was not too bad before I put brim. on it. Have to sit it out now and see how long it takes for the skin to settle again. Big bummer, as I was over the moon with my pale complexion. But if this is the standard, then the flare ups might not be worth the positive effects perhaps. Although it might also be an option to keep using the brimonidine solution every other 8-10 hours and be a step ahead of rebound flushing. The thing is though, that I am not yet certain if this stuff can cause long term damage or alterations to the facial blood vessels and I don't want to risk anything here. But the test is completed for now, it works and it has after effects. I am sad that I have to go through the busy weekend looking like this and feeling burned up, and more sad that I can't put  the brimonidine on my face at the moment, but well. Is there anyone with suggestions perhaps? It works, but why do I (others) get rebound flushing? It can't be the inactive ingredients, as there are none in my case. I would love to use this daily but am not convinced I am not making matters worse in the long run with it. Then note the responses from other forum users, including our highly valued moderator Melissa W at #113, who echoed this same experience.

4th September 2010 10:07 PM: "Thanks guys. I think the worst is already over, Will try different amounts in the near future. flushing wise. Still redness on mostly one cheek, but clear patches of skin are showing already in between and the full force flushing seems over. So I think the flushing reaction is about 8 hours or something. Perhaps about as long as the paleness reaction is, so that´s not a good thing. Don´t know either Melissa why some, like WC, are not having the rebound flushing. I do have to admit that I used the solution (similar to 0,2%) very generously on my face, and didn´t use the 2 drops, but more. So that might have added to the reaction afterwards. But only afterwards, not during the 8/10 hours of action, then I was very pale. Questions indeed. Will wait till skin is back to its old self and try again in time, as I am very impressed with how it works. Just don´t know why this rebound flushing is happening. These different amounts, 3 mg/ml brimonidine tartrate in water, was used at another evening (trying it a second time), not the same first evening, I mixed that one up in my former post, its been a good few years since already.

End verdict for me: brimonidine works and quite dramatically pales the skin. But the rebound is too severe and too long lasting to make this a workable treatment for me. There is also a lot of worry about weakening the blood vessels in the long run and potentially worsening the rosacea. I won't use brimonidine again. HERE you can read about the trials with brimonidine's big brother, Mirvaso.