My savior: Ketotifen Fumarate

I never had allergies until I moved to Oklahoma. Evidently, when the wind comes sweeping down the plain at +45 mph, its carrying billions and billions of grains of cedar pollen. So even though I grew up in a damn forest, Im now allergic to 'trees'.

*bonus* Arnie is allergic to trees AND grass.

A dog.

Allergic to trees and GRASS.


Well, the past couple springs I just suck it up, take two benadryl every night (give two to Arnie) and just deal with it. But this spring I got a new bit of allergy fun-- Itchy eyes. Im not talking 'aw balls something is in my eyes' itching, I mean 'OMFG DO I HAVE EYE CHICKEN POX SOMEONE KILL ME' itching.

Id reached my breaking point last Friday (I realized if I gouged out my eyes, they wouldnt itch anymore!), but luckily I work in a micro/immuno department, and I got some good advice: Ketotifen Fumarate.

Holy mother of god I love this stuff.

Allergies are just one of four flavors of 'inappropriate immune response' (Type I), illustrated here.

The trouble starts with a specialized immune cell called a mast cell. Mast cells dont make antibodies, but they have receptors on their cell membranes that stick to the stalk part of IgE antibodies, leaving the 'business end' of IgE sticking out from the mast cell like spikes on a sea urchin.

When an allergen gets into your system, it sticks to the 'business ends' of IgG on the mast cells, 'crosslinking' lots of IgEs together (tethering them together in close proximity). This tethering sends a message to the mast cell: "POOP OUT YOUR HISTAMINES AND JUNK!!" and *SQUISH!*, the mast cell dumps a shitload of histamines (and other stuff) into your nose/respiratory tract (hay fever) or digestive system (food allergies).

Well in my case, mast cells were pooping histamines in my eyes. Considering that there are oh, about 50 million mast cells in your eyes... there is potentially a LOT of histamine pooping going on when there is cedar pollen around.

Now histmines themselves dont cause any trouble-- theyre just the messenger. Its the target cells that cause trouble in response to the histamines. So one way ketotifen fumarate works is by competing with histamine for one of their target receptors, H1. H1 is the one that makes teh itchey. Cant deliver teh itchey message, no teh itchey.


But wait! Theres more!

Ketotifen fumarate also calms down mast cells, preventing them from pooping their guts out in the first place!

Which is great cause histamines arent the only thing in mast cell poopage. There are also other chemical messengers that tell the immune system that shit is going down. In response to these messengers, other immune cells, like eosinophils, cruse into the eye all like 'Whats all this, then?' and start pooping their chemicals out. Eosinophils poop contains toxic shit that is normally used to kill bacteria and parasites... and its toxic to your tissues too.

So ketoifen not only keeps the 'AHHHH!' message quiet by shushing up mast cells, but it ALSO tells eosinophils 'Move along. Nothing to see here.' preventing totally unnecessary tissue injury.

In summary, my eyes feel AWESOME now, because the ketoifen fumarate in the eye-drops Im using is blocking the histamine H1 receptor, inhibiting mast cell degranulation, and telling eosinophils to piss off.

Awesome, you guys. Awesome. Get this stuff if you have eye allergies-- Its OTC. You dont have to gouge out your eyeballs.


More like this

One of my favorite places on the internet is r/askscience, a place on reddit where people come and ask questions, and a panel of scientists answer. People can ask follow-up questions, and there is often some great back-and forth (to be honest, part of the reason I haven't been writing as much here…
Hay fever, as those of you who have it know, can be a most remarkable feeling. Your eyes itch, and your joints ache. You feel as though you were coming down with the flu. Time itself can seem distended, warped. Your hands feel like balls of dough, and you're sleepy. You feel…
If there were a parallel universe, and in that universe medicine, instead of being based on science, was simply a gemisch of various folkways and superstitions, medicine in that universe would be called "naturopathy". "Remember. Hey, how come this never works with water?" I've discussed the…
Every Spring, you can count on a handful of posts here at ERV on allergies. Ive got em. I hate em. But I recognize that in many ways, Im 'lucky' as far as allergies go. I only have to deal with them for a few months of the year, I can move somewhere else and not have to worry about them at all…

'(...) poop contains (...) shit (...)'

You just made my day.

By Ketil Tveiten (not verified) on 27 Apr 2009 #permalink

It all sounds so irreducibly complex.... *ducks*

You need to write a chapter summary in the next edition of Kuby Immunology.

When I was a little kid we had a dog who was severely allergic to grass. She got sick if she spent more than a few minutes outside when it wasn't winter. Had to stay inside and had to be trained to go in a specific place in the house on newspaper. Was not good.

I can so sympathize. I spent a good 16 years with no allergies and then magically my body went "HI THERE POLLEN! WE HATE U NAO!". Since then I get all hay fever and the desire to claw my eyes out for 2 months of the year. It's all made of serious suck.

Brandon-- Dogs can totally have benadryl, and store brand versions are super cheap now! Ask your vet, cause it sure helps Arnieman!

And the Ketotifen drops I got were Walmarts generic 'Equate'. $11 (still expensive to me). Name brand (Zaditor) was like $18. But those are for people, not teh puppahs. Puppah mast cells and people mast cells are different-- definitely ask vet first on this one (if thats what you meant).

I once had to deal with a horse that was allergic to grass, and not aware of it (the horse, that is).

*That* was interesting...

OMFSM! Abbie, it's not possible for me to love you any more, so I'm going to take some of this extra love you just earned and put it over by the door, K? No more itchy eyes? And Ben Stein isn't even remotely involved? â¥

Brilliant timing Abbie. I have been suffering from horrible, itchy, runny eyes for the last 3 weeks. The current love of my life keeps telling me I've developed an allergy, while I claim it's something else. Anything else.

If this fumigate stuff works then my wife is right and I'm wrong. (wouldn't be the first time)

Hi Abbie,

Has there been any research conducted on the transfer of allergy susceptibility from person to person? My wife did not suffer any allergies until after she met me which lead me to wonder whether I spread some of my IgGs to her through swapping various bodily fluids.


If ketotifen fumarate binds to H1, wouldn't that cause the same message to be transmitted as if histamine binded?

KiwilnOz: allergies can't be transferred. You really can't give someone antibodies (except maybe IgA) through saliva and copulatory fluids.

Jeremiah: lots of inhibitors bind the same molecule as the correct ligand. For instance, aspirin binds COX and prevents it from making "poop".

I suppose my question has less to do with the fact that you can infer from Abbie's description that ketotifen fumarate is an inhibitor and more to do with how exactly it inhibits: aren't there examples of competitive "inhibitors" of receptor proteins that actually cause the same message transmission as the intended molecule?

I understand how inhibitors work on run-of-the-mill enzymes, but receptors I'm a bit flaky on. As long as some molecule goes into the receptor and causes the receptor to react as if the intended molecule is binding, wouldn't the same outcome occur, e.g. teh itchy?

Thanks Dunbar. She was obviously just allergic to me.


Competitive receptor antagonists basically squeeze into the binding site preventing the correct ligand from reaching it, but don't activate the receptor as an agonist or the correct ligand would. I'm not that knowledgeable about pharmacology so I can't explain better, sorry.

Side effects include ... irritability

Oh, I pity the poor creotards, ERV is going to start being irritable!

Side effects include ... irritability

Oh, I pity the poor creotards, ERV is going to start being irritable!

I lived happily for sixteen years of life without any allergies at all. Then I moved to Australia and a whole country-load of alien pollen chuckled, rubbed its hands and said, "Your ass is grass, fucker!"

I fully sympathise with the urgent desire to remove eyeballs with fingernails. Not fun. Not fun at all.

If you think about ligand-receptor and ligand-enzyme interactions, they can both be reduced to something binding to something. They can therefore be described by the same concepts like Michaelis-Menten or Langmuir equations, for example. Concepts such as competitive, uncompetitive, and noncompetitive inhibition are also applicable if a receptor needs a co-receptor (or needs to cluster with other receptors) or say has an allosteric binding site for the inhibitor that prevents conformational change. That's my take on it anyway-- I don't have examples in mind to illustrate what I'm saying.

One addendum: many receptors are also enzymes if you think about it, because many of them have kinase domains.

Thanks Dunbar and LostMarbles. I'm too lazy to look up exactly what kind of inhibitor ketotifen fumarate is, but with possibilities like an allosteric binding site on the receptor or competitive inhibition at one of many active sites, I can at least imagine a mechanism. I appreciate the assistance =)

Thank you for this info! I'll be stopping at the Safeway on the way home for this stuff.

Also, thank you for the phrase "pooping histamines". I'll use that in conjunction with "plant sperm" when discussing my allergies from now on.

I guess it is a "family of chemists" thingie but whenever we got itchy eyes we washed them with eye cups when we came in from the great outdoors (very dilute boric acid solution).

I don't even know where you would buy an eyewash cup now.

Ours were ceramic with an eyeball embossed on the side.

By Prometheus (not verified) on 29 Apr 2009 #permalink

Prometheus, the best bet for finding eye cups would be antique stores and flea markets. They come in many handsome shades of glass. I suppose some people collect them because some people collect pretty much everything.

I had about a 15-year holiday from allergies when I first moved to California from Pennsylvania. Then they came back with a vengeance, cost me my best work ever (I was a specialty arborist) and over the years got more and more annoying.

I've perforce done some research on urban trees and recent history. My personal nemesis is a mulberry cultivar, 'Fruitless', and maybe a brother cultivar or two, that is one of the kinds planted in North American cities over the last century as so many elms were done in by Dutch elm disease.

One ideal was to plant an urban tree that was not "messy." Mulberries are tough, heat-tolerant, deciduous (therefore ideal for moderating sun on the south exposure of a building) and I think good-looking. The "problem" is the berries.

I grew up with a mulberry in the neighborhood; it was our gathering place, playhouse, climbing gadget, and snack bar. (I thought of her as a friend but then I'm a weird treehugger.) Mulberries are delicious. These were purple. This was in the '50s when most folks used clotheslines. Purple children, purple-spotted sheets (bird traffic)âyou can imagine. But really, that was minor and very seasonal.

So, somebody got the bright idea of cloning mulberry twigs with male flowers only into male-flower-only trees, ergo no messy fruit. Mulberry flowers are relatively inconspicuous catkin-looking thing because they don't need to attract pollinators; they're wind-pollinated. Small, lightweight, pollen grains: they look like cigarette smoke curling off the flowers when they're turned loose.

There are five blocks on our street, including ours, planted with 'Fruitless' mulberries. We've lived in this duplex for going on 14 years. I garden. I sit on the front porch and watch the birds, evenings. I work at home.

This year, maybe two days after the mulberries bloomed (profusely; almost everything is, this year), I ended up in the ER getting the standard X-rays and arterial stick and such and snorting albuterol and steroids and getting a nice IV bolus of more steroids and then spent the next week-and-a-half gulping lots of prednisone and a buffet of other nice chemicals. I'm still in the process of tapering off. I've met some very nice specialists. Obviously I'm going back to the allergist for tree shots this year.

And it's largely because of some '50s ideal of Good Housekeeping: no mess, no female wet stuff, just nice clean spermy drift in the air and we haven't figured out that problem yet so it's perfect.

Ever read those old issues of Life magazine about the promises of the peaceful domestic atom? Personal rocketpacks, self-cleaning kitchens, yadda yadda? Don't you miss that kind of optimism?

It's actually illegal to plant 'Fruitless' mulberry in some cities in Arizona, Nevada, and California now, they've caused so many problems to so many people. What's planted in your city? Urban trees are absolutely great: so much habitat, weather mitigation, air filtering, long list of et ceterae. Guess every process needs thoughtful refinement, dammit.

And I'm off to find those eyedrops. Thanks!

@Holy Schmidt - Melanie: This post may have saved a friend of mine, too. I forwarded this post to her, since she has been miserable with itchy eyes, etc. She bought the eyedrops and oral meds today and feels so much better.

@ERV: you need to get a big Pharma check for this advice. :)

Prometheus: I was down the chemist's the other day to buy antihistamine-flavoured eye drops (which have been helping a bit but not completely) and noticed a box of blue plastic eye baths on the shelf. Actually what I noticed first was the price tag: 10c (Australian). Cheapest item in the shop, clearly intended as single-use items. I've seen glass ones in my youth, fancy Victorian ceramic ones on the Antiques Roadshow, and there ought to be a few disposables in every first aid kit.

By John Scanlon FCD (not verified) on 30 Apr 2009 #permalink

I've suffered from springtime hayfever itchy eyes for years. I've had bad experiences with antihistamines (severe drowsiness) so I've decided to just suffer instead. When I saw this post, I went down to the local CVS and found some ketotifen drops but didn't bother trying them until just today (nearly continuous rain for the past two weeks has kept pollen down) but it started clearing, itching returned, so I applied the drops and voila! works as advertised and no drowsiness!

So, thank you Abbie!

By Sean McCorkle (not verified) on 09 May 2009 #permalink

I know I'm a little late, but thank you thank you thank you! This stuff is great! I just started having bad eye allergies this year and thus far these drops are stopping it completely!

I have a 96 yr.old man who lives with me who lost his home in katrina .He is from ms.I have been his nurse for 11 yrs.He has been having lots of allergies.His eyes have been red-red-red with pus.I tried everything.Thank God his doctor prescribed Ketotifen.It,s absolutely unbelievable.A true miracle.Thanks keto for all your hard work.Blessed in ala.

By blessed in ala. (not verified) on 29 Mar 2010 #permalink