17 September, 2017

Montelukast (Singulair) for rosacea flushing and redness

My dermatologist suggested lately that I could try out an asthma/allergy med called Montelukast (brand name Singulair). I was already given it last year coincidentally by my GP for my bronchitis at the time, but never took it very long. My dermatologist said that singulair is helping some of his rosacea patients, especially flushers, as it is supposed to lower inflammation and interferes with mast cell issues, which can play a role in allergies and flushing. Singulair (this is the brand name, the generic active ingredient MONTELUKAST is just as good and what makes it work) is designed to treat asthma inflammation in the lungs. It also prevents the narrowing of airways triggered by exercise. Singulair is a leukotriene receptor antagonists. It works by blocking substances in your lungs called leukotrienes that cause narrowing and swelling of airways. Blocking leukotrienes improves asthma symptoms and helps prevent asthma attacks.

Leukotrienes are also involved in rosacea flushing and skin inflammation however. Leukotrienes are a family of certain inflammatory mediators produced in leukocytes in the body. They play a role in the regulation of the immune responses in the body. But when leukotrienes are produced, they also stimulate the production of histamine (which is a blood vessel dilator and also involved in allergic reactions), as well as the production of prostaglandins. There are 'good' and 'bad' prostaglandins and the body. The BAD ones create inflammation and pain. They also play a role for instance in the painful inflammatory response in the uterus when women menstruate. This is why NSAID's, which control the prostaglandin production, can really help with menstruation pain; they make sure there are less of these bad prostaglandins produced by the body and this lowers inflammation and pain. Bad prostaglandins are bad news for rosacea, as they cause inflammation of the skin. They can cause facial flushing. Increased levels of prostaglandin D2 make the skin look red and inflamed. (By the way, certain foods, especially sugar and white flours, also raise the levels of prostaglandin D2 in the body and skin). Unfortunately, research tests showed that taking a prostaglandin D2 (PGD2) receptor subtype 1 antagonist (laropiprant) (to counteract the levels of prostaglandin D2) did not improve rosacea subtype 1 symptoms. Still, inhibiting even some of the leukotrienes is beneficial, and many rosaceans have reported that leukotriene blockers help decrease the inflammation associated with their rosacea. As illustration: Doctors have used an antibiotic called azithromycin effectively in the treatment of occular and regular rosacea, and one of the ways in which it helps rosacea, is in the way azithromycin lessens certain  pro-inflammatory cytokines in the body (including IL-1, IL-6, IL-8, IL-10, and TNF-α), and because it down-regulates the production of nuclear factor (NF) kappaB and of leukotriene B4.

One of the roles of leukotrienes (specifically of leukotriene D4) in asthma is to contract the smooth muscles lining the smaller parts of the lungs. Of too many leukotrienes are produced by the body, they cause a lot of inflammation in asthma and allergic rhinitis. Leukotriene antagonists like singulair/montelukast are used to treat these disorders, by lowering the production or activity of leukotrienes. Cysteinyl leukotriene receptors are present on mast cells, eosinophil, and endothelial cells. They can stimulate pro-inflammatory activities by mast cells. They can create inflammation, induce asthma and other inflammatory disorders, thereby reducing the airflow to the lungs. Cysteinyl leukotrienes seem to also play a role in adverse drug reactions in general.

So, despite singulair/ montelukast being developed to treat asthma symptoms, the way in which it lowers specific chemicals (leukotrienes, prostaglandins, histamine),which also play a role in rosacea inflammation, means that it might also help some people with rosacea and with general skin redness and flushing. 

I am glad to try it out and have already taken it for a few weeks, but too soon to tell if it improves matters. Some days I think it does, others I am not so sure. Hopefully better effects in weeks to come. One of the known side effects is increase anxiety or jitteryness. I have not felt as calm as normal lately, but these things can be hard to pinpoint to one specific cause. I know of two other rosacea patients who currently try singulair out, and both of them are in the same boat, not being sure whether or not it helps or not. Ginaisred for instance, and she wrote about it on The Rosacea Forum: "Hi all, thought I would start a new thread to discuss Montelukast. I know some people on this forum are patients of Professor Anthony Chu at Hammersmith, and he has recently advised us flushers to start using Montelukast. I thought I would create a post to keep you updated and anyone else who is trialing it please add in your thoughts.. So far: I have been on it for a week - sadly no improvements yet. I assume it may take a while if it was to work?  Fingers crossed for me."

Singulair has been used by rosacea patients in the past already too
and some wrote reviews. let's have a look what they thought about it. All reviews are found on public forums and websites, and under 'wrote' (behind user names) are links to the exact source.

YankeesRtheBest wrote on May 11th, 2007:  "Singulair is amazing..I have been on singulair for about 2 months now and it has been excellent at keeping my Rosacea under control. My flushing has been non-existent. Even the terrible night flushes and exercise-induced flushing has subsided. I started singulair because I tested positive for allergies (tree pollen, dust mites) I started getting allergy shots and my allergist also prescribed me the Singulair. What is even more amazing is that my broken blood vessels are much less noticeable than they were and my chronic redness is at least 50 percent better. I strongly recommend this, however I'm not sure how you can get it prescribed for you if you don't have allergies or asthma. he only thing that hasn't been helped much is my ocular rosacea. Hope this info helps. [..] I am on 10 mg. I noticed that my Rosacea was significantly better after about 4 or 5 weeks. Now, after 2 months of being on it, my flushing has been diminished to almost non-existent. And yes, even my emotional/social nervousness flushes and indoor heat flushing has been helped tremendously. I don't know if this would be the case for everyone, but Singulair def seems like a wonderful option for people to try. Good luck. -Chris"

Froggirl replied: "Thanks for this info, it's so interesting, at first I assumed singulair was a type of antihistamine (which I'm already on) but it's completely different...as far as I can tell from googling it's usually used for asthma, not for skin reactions, although I found one reference that said it possibly could help skin allergies. So I'm really curious to know if your doctor prescribe it for asthma or skin allergies? I did some more googling and it is used for mastocytosis, which is a disease where the mast cells degranulate too easily, and so causes extreme allergy type reactions, including flushing and wheezing. I'm being checked out for this at the moment because everyday now I'm flushing all over and having wheezing attacks (but have no allergies). [..] Despite it being unclear what triggers rosacea in the first place it's pretty clear that the symptoms are related to inflammation, and leukotriene's are one of the inflammatory mediators that contribute to inflammation, along with histamine and prostaglandins etc. So potentially blocking any of these inflammatory substances could reduce the inflammation and improve rosacea. In allergies the release of these chemicals is due to the immune system overacting to common substances, but the end result is that the same chemicals get released, causing redness, swelling and warmth. And then the inflammation caused by these chemicals trigger the release of more chemicals and things can just get worse and worse. So even though the initial trigger for the inflammation may differ between rosacea and allergies the same treatments can potentially help both."

Froggirl updated on June 1st 2007: "I'm up to 9 days and the last few days my asthma has been much better and my flushings has maybe been a bit less but nothing dramatic. Saw my doctor today and he said it does start to kick in for asthma after 7 days and gets to the full effect at about 2 months so i assume it will be a similar story for flushing."

Melissa W wrote on May 12th, 2007: "In Nov (2006) I asked my derm to put me on singulair because I had read (I think in Nase's book) that it may help with rosacea. I also happen to have asthma. I developed it 7 years ago along with all my other allergies which appeared all of a sudden but then my asthma mysteriously disappeared about 2 and 1/2 years ago. Anyway, I have noticed no change in my rosacea due to singulair but I am currently still on it because my derm said there are no negative side effects from it (a safe drug) and also because I still have so many allergies."

YankeesRtheBest updated on June 8th 2007: "I would defenitively give the singulair a while to work. I noticed that my flushing was 95 percent gone after about 2 months. It all has to do with the inflammatory leukotrienes. I spoke to my allergist about this. I told him how my rosacea was so much better after being on the singulair for a couple months and he explained to me that inflammatory leukotrienes are the reason for different types of inflammation such as in the reaction to allergies or asthma. He said inflammatory leukotrienes are also in the blood vessels. Singulair helps release these leukotrienes from the vessels. This could be why it helps the flushing of rosacea and also why my broken blood vessels appear to be less visible. But yea...def give it a couple months. Don't give up on it too soon. Good luck. -Chris"

Barbara wrote on June 10th 2007: "I’m 3 weeks on Singulair now. Still no results for flushing. I really hope I will see some first results in the next 2 weeks. After stopping my antidepressant some time ago my flushing slowly has come back to the same distressing strength than before taking the antidepressant, so I’m so desperately hoping that Singulair will help! The last 2 weeks I had some minor belly ache. Could be from Singulair as it is listed as one of the most possible side effects. But it is only minor, so no reason to stop taking it. Take care all, Barbara"

She updated on July 25th 2007: "Update: So I stopped taking Singulair last week on wednesday. On Sunday evening and the whole Monday a was quite flushy and my face got redder again and still is. The last weeks while taking Singulair I was much "cooler" and pale. I really thougt that this was because of summer, when I don't flush so often. But after stopping Singulair I have the feeling that it acctually may have helped me. HHMMMM...it's always so difficult to tell if this flushy time would have also happened if I would still be on Singulair."

And she updated on September 26th 2007: "I started my second Singulair trial 4 weeks ago. And this time I not only can say for sure that it is really helping, moreover it started helping already the next day after taking the first tablet. I took the first tablet in the morning. When I got up the next morning and looked into the mirror I thought: “Wow, I look so pale, but that can’t be because of Singulair, I just took the first tablet yesterday!?”. But it’s true, I am really paler since taking Singulair and the threshold for flushing is noticeable higher than it would be at this time of the year. Two colleges at work already asked me if I would feel sick because I look so pale! Don’t get me wrong. I still suffer from frequent mild up to strong flushes depending on the trigger. It is just in compare to not taking Singulair that I feel better. Singulair just puts the threshold higher before a flush starts. I would say it saves me from a lot of mild flushes and helps my face to stay a little bit “cooler”. But the most noticeable result from Singulair is my paler face. It is not a cure though but every little relief is highly welcome. And because Singulair works against inflammation I assume it may slow down the progression of rosacea in general, or at least I hope so. However I feel far from being able to live my life in a fairly “normal” way. This flushing/blushing thing is draining so much joy and energy out of me. I feel sooo tired. Just to think how happy I am that I have perhaps one flush less a day because of taking Singulair shows me how desperate I am.   Sorry for whining. I really started that post with another intention. Best wishes, Barbara"

Barbara further updated on December 1st 2007: "I just want to give an update on my treatment with Singulair. I take it daily since August now and it is still helping me to paler and cooler face. In autumn/winter I normally have a lot of mild or strong flushes during the day depending on the trigger and often nose flushes during the night. This time Singulair helps keep away many of the mild flushes and the nose flushing during the night. And it definitely helps reducing the flush when I come from the cold outside into a warm room. However; it is only helping to some degree…if the trigger is strong enough I still have my strong flushes. Especially the ones that come from anxiety, embarrassment and warm indoor heating. But I’m thankful for every flush that I don’t have, even if it would have been “only” a mild one. So far I don’t have any negative side effects from Singulair that I’m aware of. It is just soo expensive!!"

iVAN wrote on June 17th 2007: "Been on Singulair for 5 weeks and have no improvements in any rosacea or flushing symptoms. Actually I don't notice it doing anything at all so far."

Twickle Purple wrote on June 20th 2007: "Within days of starting Singulaire my face was cooler, and now I flush much less. My face is almost always cool to the touch. My triggers are mostly allergy related and the Singulaire has worked great. I take it with a reactine and a zantac in the morning."

She updated on September 27th 2007: "I urge anyone taking this to be aware of the side effects. This drug helped me SO MUCH but I had to stop taking it because of the horrible side effects I was experiencing. Check this out: http://www.medications.com/singulair/browse I have been off the Singulair for over 3 weeks now and am finally feeling better. The deep pain and ache side effects slowly went away within the first week and by the second week I was left with just generalized weakness but no more pain. In my third week my strength was coming back, I could hold a full teapot, but I had no stamina even for a short walk. Now I am starting my 4th week post-Singulair and I am getting some vigor back. I went for my first walk yesterday and was able to walk at a gentle pace for about 20 minutes -- no hills or inclines though, I'm not up to that just yet. I am saddened that such a helpful medication could rob me of my life-force like Singulair did."

Froggirl updated on June 21st 2007: "I wonder then if it works best taken with antihistamines? Because as far I as know leukotrienes are unlikely to be released in the body on their own but in tandem with histamine (and the other mast cell contents), meaning that if you take just singulair the histamine may still effects the blood vessels anyway..Similair to how H1 antihistamine didn't make much of difference to my flushing but taking a combination of H1 and H2 did. I've been on sigulair over a month now and my facial flushing is improved, not gone by any means but it is noticeably better and i'm hopeful them it might improve even more over the next month.

Max wrote on June 21st 2007: "No noticeable results for me after 3 weeks on singulair..."

Liz wrote on July 16th 2007: "Been taking singulair for 3 weeks now... face is still covered in hives, red and swollen... with some nice deep sores added for extra misery. All singulair has done was take about $100 out of my wallet for copays. Should i give it another month? what do you think? - liz"

Kathy S. wrote on July 25th 2007: "Singulair wasn't amazing for me. I only took it for a little over a week but it made me irritable and shaky, some little panic attacks, it was really weird. I took it with zyrtec. Also it didn't help with my flushing, I believe it got worse. I hope that others are really seeing help from it. I just didn't get the results and couldn't take something that made me stress more as that is my biggest cuprit and wind."

Alba wrote on January 29th 2008: "I just started singulair 2 days ago, i think its already working have been flushing less often."

dwit392 wrote on February 15th 2008: "When I combined Singulair and Zyrtec I seemed to get amazing results. I don't believe I got the results with Singulair alone (I took my prescription in two parts of 15 days each) I didn't really realize until I stopped taking Singulair how much it was helping me. I need a new prescription now. It seemed to greatly reduce my internal heat. My redness was down 25%, flushing threshold was about 20% higher, and I stopped getting those annoying evening flushes, due to dry air or internal heat or whatever. Only thing strange about singulair is that I had to take it right before I went to bed because if I took it in the afternoon it seemed to induce a flush. I take 10 mg once per day before bed. I usually take it without food. I dont think it really matters."

Mutantfrog wrote on February 18th 2010: "I've been taking Singulair for about 10 days now, and I'm starting to see some improvements already. My flushing response has been WAY down. The 2 times I have really flushed in the last 5 days (which is amazing in of itself) the flushes were significantly shorter in duration. I was told singulair typically takes about 2 weeks to start working well, so I was surprised to see this difference already. I keep a photo journal of my progress, so that I can tell when rx/ipl and such change one way or the other - hopefully making things a little less suggestive. I haven't experienced any real side effects yet. Though I'm on the lookout, thanks to the other posts in this thread. I was prescribed it for allergies/mild persistent asthma, but it will be a really nice side effect if it helps the rosacea too. [..]  My skin...still flushes. I still have the a few P&P. But the flushes haven't been quite as intense, or as frequent. I've even been able to drop the topical for my skin (Klaron) about 2 wks ago - skin hasn't looked significantly better/worse but the point is it didn't FLARE like it usually does after stopping the topical. Nice to be able to drop something more from my routine. [..] The burning/easy irritation of my skin is SIGNIFICANTLY better than 3 or 4 months ago. I just don't flush as easily in the last 3 weeks or so. I've even been able to add in some foods I normally can't eat due to flushing - and have had little to no reaction. Heat (dry heat especially) still gets me pretty red but the flushes go away pretty quickly (about 1hr vs all day), hurt less and spawn fewer bumps (I always get bumps after being really red - and they show up only in the "rosacea red" areas of my face)."

Queta wrote on July 17th 2010: "Hi- I tried Singulair quite awhile ago for nasal/cheek swelling related to allergies. I took it for about a month. It didn't seem to make a radical difference, but it made me angry. I was very short-tempered and angry after about a week of taking it. Finally after a few weeks of being unusually angry I looked it up and a small number of people report the same experience. One guy even told about how he and his wife divorced because her attitude completely changed after taking it. I'm sure that's only a portion of that story but I will say it affected my mood a lot. No one else on here has reported that effect, as far as I can tell. Regards Queta"

Mrsmoof wrote on october 11th 2010: "6 1/2 weeks on Singulair.. Haven't noticed much of a difference. I have noticed though my neck and face seem a little cooler. Redness, flushing still about the same. Will give it 3 months."

Snuffleupagus wrote on October 11th 2012: "Is it possible for Singulair to make flushing WORSE? I took it for two nights and I had horrible "centre flushes" causing me to wake up in the middle of the night. (not like a regular whole cheek flush, but focused more in one area and VERY red/purple!) Wondering if this is just a coincidence (I have been getting these on and off constantly over the last 6 months)."

Cricket0117 wrote on April 30th 2013: "I started taking Singulair last week Friday, sat morning when I got up my face turned a little pink instead of the red and burning I've had for the last 4 months. I have not had any major flares or burning since then. My face is far from perfect but it's improved from what I've been dealing with.Has anyone had similar results and has taken it long term with good results."

lm4727 wrote on May 26th 2014: "Hi all, Both Singulair and anti-histamines made a dramatic difference for my skin (flushing, redness, hives), but I had to stop both because they made me tired and sluggish. I would recommend Singulair to anyone who doesn't have side effects from it. Two zyrtec per day did the trick for me as well, but I can't take these drugs for any extended period of time."

Ginaisred wrote on March 3rd 2018: "Hi, according to Prof Chu (who is well known in the Rosacea / acne field) I trust him hugely, there are no side effects with Montelukast. However, you never know. I now take 20g of Montelukast at night and the one thing I have noticed is I wake up with a stuffy nose.. Perhaps that is due to the cold though, I cant be certain. I think it makes me slightly tired too, although most allergy medication would do. For some, montelukast has been amazing. I have not seen any benefits yet."

Rednessator wrote on March 14th 2018: "Last monday, that is, 8 days ago, I upped my Zyrtec dose to 10 mg in the morning and 10 mg in the evening. I felt a burning sensation on my scalp (I have bad psoriasis like scalp problems which my derm suspects is folliculitis decalvans, but I don't know) and a sensation in my body that I'm at the burst of flushing all the time. Weird. Next day I went to my GP and got a prescription for Singulair, so Tuesday 18:00 (last week) I took my first Singulair tablet, alongside with the 10mgx2 Zyrtec I started the day before. Now, the results were pretty insane. Already the next day, I could see results on my nose. Noticeably less red. And it just continued. I've had the most amazing days until Tuesday, with a perfectly white nose. All the visible blood vessels just went away. BUT, that was until yesterday, 7-8 days after. I woke up, with a slightly red nose. My eye symptoms just went berserk during the day. I could barely keep them open, they were so sore. And my nose got redder. Same red nose this morning.  I really, really wonder what just happened...
EDIT: Monday, the day before the relapse, I fasted. I also changed bed sheets etc. I worked long hours, but did not feel stressed. I had a brilliant night of sleep...
EDIT2: Other factors that changed. I used cortisone on my inflamed scalp before I went to bed."

Rednessator wrote on March 15th 2018: "I've used 10mg a day of Montelukast for the last 5 weeks, and apart from the first week, I have not seen any change in symptoms. That first good week could also be due to the fact that I upped my zyrtec dose to 10mg twice a day. I've had my GP take blood work to test for helicobacter pylori, and he says if that is positive I have to go to the hospital for a breath test. Apparently one could not see if one is currently infected with hp, only if one has ever been infected at one point - the first being a subset of the latter. Anyway, journey continues, do not think Montelukast was my saviour."

Phlika29 wrote on May 29th 2018: "I have recently seen professor Chu at Chiswick and along with my usual laser I was prescribed singular. The first few days my face was pale but from them on it just looked blotchy = part pale and part red. I would switch in an instant from pale to bright red but my skin felt cool to the touch. I often felt like i was flushing but my face looked quite cool yet if I bent down it went redder than usual. I also felt my broken veins worsened slightly to the point I decided to stop after one month. So whilst I didn't get any real side effects from singular I felt it's effects were a little erratic for me and overall didn't help enough to keep going.  I am back for more laser soon and will update professor Chu on the singular."

Rednessator wrote on May 30th 2018: "Montelukast (singular) also did not work for me due to side effects. It does seem to have common side effects as well, and there are some concerns about it amongst parents whose children are prescribed it for asthma."

Montelukast has also been tested on acne patients with good results. 52 patients with moderate acne were evaluated and divided in test groups. One group received doxycycline 100 mg/day plus 1% Clindamycin solution (Group 1), the other group was given Montelukast 5 mg daily plus 1% clindamycin solution (Group 2). Montelukast turned out to be as effective as the antibiotic doxycycline in the treatment of acne after a three month trial, although the effects of the clindamycin solution might have also added to the success perhaps. 

Singulair is not the only mast cell related medication I have used so far. In the past I had some success with a trio of medications that are used for mastocytosis

You can read about the background info on it, and my experience at the time in this blog post. I took 2 different antihistamine medications on top for a month: Inorial and zaditine. They initially really helped me quite a lot to cut down on the facial flushing and redness. I literally looked pale some weeks, and thought I found the holy grail. But after a month or so, I felt I became more red and more easily flushed, possibly because they made my skin more dry. More than normal, at some point! I am wondering if my body maybe compensated and started producing more histamine than normal perhaps. I remember an old forum member called Dan warning for this phenomenon when taking high doses of antihistamines for rosacea... I therefore no longer use Inorial and zaditine (but still use Xyzal daily), only when I can't get out of some dinner party invite and know I will have to eat foods high in histamine. For occasional use I get relief from them therefore. However, for those who have mastocytosis, these drugs can really help. I also am eager to restart them and just see if the same thing happens second time round. I see my local dermatologist soon from now and will ask for a new trial with these meds.

In 2016 I used Tilade, which is also a mast cell, anti-inflammatory substance for the lungs

Tilade inhaler 2mg (CFC-Free) contains nedocromil sodium which is a non-steroidal agent, with anti-inflammatory properties, that reduces inflammation by a mechanism that is different to asthma medications containing corticosteroids (not to be taken when you have rosacea!). Tilade inhaler works directly on the airway walls to reduce inflammatory reactions, by inhibiting the activation of several inflammatory cells (such as macrophages and mast cells) at the site of inflammation in the lungs and preventing them releasing chemicals (like histamine, prostaglandin and leukotrienes) that mediate the inflammatory process. Tilade stabilizes mast cells (linked to allergies) and reduces the release of histamine and inflammation (by reducing the total number of eosinophils). The overall effect is to dampen down the inflammatory process in the airways, reducing irritation and swelling to improve airflow into the lungs. This helps to prevent symptoms of asthma caused by swollen and inflamed airways, like wheezing, cough, tightness of the chest and shortness of breath. It does not relieve bronchospasm which happens during an asthma attack and needs a “reliever” medication to open the airways. 

So I used it for a month or more and it helped me calm down the bronchitis and also made my skin very calm and pale-ish for a while. Until it made me more red and flushed as well, after the one month mark. Just like the mastocytosis medication! After a while of using it twice daily, I felt I needed more and more of it, or else I'd turn very red once the half life was exceeded too much and it stopped working. I assume it was some sort of rebound. I am a severe flusher and even a sneeze attack makes me all red, so as I write often, this isn't how everybody with rosacea will/would respond to Tilade most likely. Besides, it's not aimed at rosacea, I just noticed a pale skin while taking it for lung inflammation. So.. I used it a full month. And within the 3rd week I started noticing that about 6 or so hours after using the inhaler, I had what felt like a weird rebound flaring, flushing and burning?? All red! I stopped the inhaler, had 4 days of all round terrible burned up skin, cancelled all my going out plans and grumped it out. Then it subsided a bit, and I restarted that Tilade puffer, just to see if it really was the inhaler in my case. And the same thing happened. Pale that afternoon (yesss!), then super red after not snorting the next dose.  Pictures were while using Tilade and when it still made my skin calm, then last one when it stopped doing that: 

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