Antihistamines Improve T2Diabetes.

Have you tried Ketotifen?

  • Yes, for allergies/mast cell issues.

    Votes: 2 28.6%
  • Yes, for improving leaky gut.

    Votes: 1 14.3%
  • No.

    Votes: 5 71.4%

  • Total voters
    7

Remy

Administrator
Ketotifen is not a well known antihistamine in the US outside of mast cell forums...but it's a great antihistamine because it also works as a mast cell stabilizer. It's available in the US from compounding pharmacies.

And here is 2015 research showing that histamine plays a role in insulin resistance and obesity. These conditions were improved by the addition of 1 mg/day of ketotifen.

Some doctors think ketotifen will also improve leaky gut symptoms if taken 30 minutes before eating.

http://www.collegepharmacy.com/images/download/Woeller_Ketotifen_Protocol.pdf

I am taking ketotifen, though have only been taking 1 mg/day. I'm going to up it to twice a day.

Has anyone else tried ketotifen?

J Diabetes Complications. 2015 Apr;29(3):427-32. doi: 10.1016/j.jdiacomp.2015.01.013. Epub 2015 Feb 7.
Effect of ketotifen in obese patients with type 2 diabetes mellitus.

El-Haggar SM1, Farrag WF2, Kotkata FA3.

Abstract

AIM:


Mast cells are found to be an important contributor in obesity induced insulin resistance. We evaluate the effect of ketotifen in obese patient with type 2 diabetes (T2DM) treated with glimepiride.
METHOD:

In a randomized controlled study we recruited forty-eight obese patients with T2DM from Internal Medicine Department at Tanta University Hospital, Egypt. They were classified into three groups: group 1, those who received glimepiride (GL) 3mg/d alone; group 2, those who received GL 3mg/d+ketotifen 1mg once daily; and group 3, those who received GL 3mg/d+ketotifen 1mg twice daily. Fasting blood samples were obtained before and 12weeks after treatment for biochemical analysis of glycemic and inflammatory biomarkers. Data were statistically analyzed by paired Student's t-test and one way analysis of variance; p<0.05 was considered statistically significant.
RESULTS:

The obtained data suggested that the addition of ketotifen in twice daily dose has a beneficial effect on all measured parameters except adiponectin. However, glimepiride plus ketotifen once daily only affected the level of inflammatory biomarkers without any significant effect on other parameters.
CONCLUSIONS:

The co-administration of ketotifen twice daily plus glimepiride improves glycemic and inflammatory process in obese patients with T2DM.
Copyright © 2015 Elsevier Inc. All rights reserved.
 

Upgrayedd

Active Member
I wasn't familiar with ketotifen, but a google search tells me its the same antihistamine found in Zaditor eye drops, which I have used for eye allergies. I wonder if the eye drops have any of the mast stabilizing effects as well...
 

Remy

Administrator
My MC issues are relatively mild. I've had good luck w/ royal jelly.
I also love Royal jelly.

But wouldn't it be something if your "mild" mast cell issues were actually responsible for your more severe symptoms too (even if seemingly unrelated)?

I just found out today that mast cells can stimulate prolactin release. I've been chasing down the root cause of that mildly elevated prolactin for years now. Could it be that it was the mast cells all along?
 

Remy

Administrator
I'm totally wrong about Ketotifin which is Zyrtec. I think I have that for allergies and it's not sedating for me. I was thinking of atarax. @Remy isn't that OTC?

@Strike me lucky For you!

View attachment 1313
Love the Guinea!

Ketotifen is Zaditor. It's rx only in the US and available only through a compounding pharmacy.

Zyrtec is cetirizine. I like it as an antihistamine a lot but it doesn't have the same mast cell stabilizing properties as ketotifen. Ketotifen is more sedating though, but it does wear off after a week or two.

Atarax is another good antihistamine but first generation vs Zyrtec which is second generation. The second gen antihistamines don't tend to cause as much sedation. But the first gens tend to work better in some cases still. Atarax makes me super groggy the next day. I've never taken it enough days in a row to see if that effect passes like it did with the ketotifen.
 

Who Me?

Well-Known Member
Love the Guinea!

Ketotifen is Zaditor. It's rx only in the US and available only through a compounding pharmacy.

Zyrtec is cetirizine. I like it as an antihistamine a lot but it doesn't have the same mast cell stabilizing properties as ketotifen. Ketotifen is more sedating though, but it does wear off after a week or two.

Atarax is another good antihistamine but first generation vs Zyrtec which is second generation. The second gen antihistamines don't tend to cause as much sedation. But the first gens tend to work better in some cases still. Atarax makes me super groggy the next day. I've never taken it enough days in a row to see if that effect passes like it did with the ketotifen.
Yah Atarax had me really drugged the next day. I do have another one, I can't remember the name, to try. I think I have zyrtec for allergies but it wasn't sedating.

I have periactin to try.
 

Who Me?

Well-Known Member
Love the Guinea!

Ketotifen is Zaditor. It's rx only in the US and available only through a compounding pharmacy.

Zyrtec is cetirizine. I like it as an antihistamine a lot but it doesn't have the same mast cell stabilizing properties as ketotifen. Ketotifen is more sedating though, but it does wear off after a week or two.

Atarax is another good antihistamine but first generation vs Zyrtec which is second generation. The second gen antihistamines don't tend to cause as much sedation. But the first gens tend to work better in some cases still. Atarax makes me super groggy the next day. I've never taken it enough days in a row to see if that effect passes like it did with the ketotifen.
Yah Atarax had me really drugged the next day. I do have another one, I can't remember the name, to try. I think I have zyrtec for allergies but it wasn't sedating.

I have periactin to try.
 

Cort

Founder of Health Rising and Phoenix Rising
Staff member
About 4 years ago I did a blog on the preliminary results from a Ketiotifen trial and did an overview of mast cell activation in fibromyalgia
Of course by now I had forgotten all about what MCAS is :bag:

1990 and 1997 skin studies found high levels of IgG deposits in the skin that appeared to be caused by mast cell activity. Nine years later a 2008 FM study suggesting immune problems in fibromyalgia pointed an arrow at mast cells, but it wasn’t until 2010 that a Spanish FM study looked again at the skin – and found greatly increased levels of mast cells in the skin of every FM patient tested – a high positive rate for any disorder.

At that point, Ang, a frustrated physician/researcher not happy with a 30% success rate for FM approved drugs got busy. When preliminary results from his small NIH funded Ketiotifen FM study suggested the drug was working; he stated “I am quite excited. I think we are on the right track. The most rewarding thing I think that I can tell you being a physician scientist, is hearing from patients that they are responding to the medication that we are testing.”

One patient who didn’t know but assumed she was on the medication was pain free for the first time in years; “I was sure I had medicine, not the placebo. I was pain free. It was amazing. I was like I can’t believe this, I think they’re on to something.”

....Ang, the leader of the study thought

“So my hypothesis is that if we quiet these immune cells then it will not send too many signals to the peripheral nerve endings and therefore would lessen the transmission of signals or pain to the brain and spinal chord and hopefully reduce the overall pain”



But Theoharides did not think ketiotifen was the cat's meow for mast cell activation


"Thus far preliminary results suggest Ketiotifen may be helping in Fibromyalgia but Theoharides, believes better mast cell ‘stabilizers’ are available. Ketiotifen, he reports, is effective at blocking the release of allergy producing immune factors but does not block pro-inflammatory cytokines, which he believes are key in ME/CFS and other disorders.
Theoharides 2012 study found that quercetin and luteolin were more effective than cromolyn, a mast cell stabilizer, at reducing cytokine release and he’s produced a patent-protected neutraceutical product called Neuroprotek (available without prescription) he believes will work better. The problem with many neutraceuticals is getting enough of their active factors into the system to make a difference. Theoharides believes using olive kernel oil in his products significantly increases the flavinoids availability."


In 2014 the results of Ang's study were released and the study basically failed.

Clin J Pain. 2014 Nov 3. [Epub ahead of print]Mast Cell Stabilizer (Ketotifen) in Fibromyalgia: Phase 1 Randomized Controlled Clinical Trial.
Ang DC1, Hilligoss J, Stump T.
OBJECTIVES::

Compared to healthy controls, patients with fibromyalgia (FM) have more mast cells in the skin. Whether mast cells are involved in the pathogenesis of FM is unclear. We sought to determine the effects of a mast cell stabilizer (ketotifen) on FM symptoms.
METHODS::

Fifty-one FM subjects were randomized to daily oral ketotifen 2 mg BID (n=24) for 8 weeks or placebo (N=27). Mean age of subjects was 51.2 years (standard deviation/SD 8.4); 88% were female and 88% were white; 22% were taking concomitant opiates; and mean pressure pain sensitivity (range 0-20) was 10.0 (0.4). At study entry, the weekly average pain intensity was 6.4 (1.1) and the mean score on the Revised Fibromyalgia Impact Questionnaire (FIQR) was 66.8 (14.0).
RESULTS::

We found no statistically significant treatment group differences from baseline in either group for the two primary measures: weekly average pain intensity [ketotifen -1.3 (1.9) vs. placebo -1.5 (1.9), P=0.7]; and FIQR score [-12.1 (19.5) vs. -12.2 (18.1), P=0.9]. No secondary outcome measures (BPI pain intensity, and pressure pain sensitivity) reached statistical significance; results did not differ in the intent-to-treat and completer analyses. Other than transient sedation [6 (28.6%) vs. 1 (4.0%)], ketotifen was well tolerated.
DISCUSSION::

The study results question whether skin mast cells play a major role in the pathogenesis of FM. However, given the role of mast cells in peripheral and central nociception, and the minimal side effects of ketotifen, a randomized clinical trial using increasing doses of ketotifen may be warranted.
 
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Remy

Administrator
Theoharides 2012 study found that quercetin and luteolin were more effective than cromolyn, a mast cell stabilizer, at reducing cytokine release and he’s produced a patent-protected neutraceutical product called Neuroprotek (available without prescription) he believes will work better.
Don't you think maybe this says it all?

2 mg of ketotifen is probably not nearly enough. Most I've read suggests higher doses are more effective. I'm on 1 mg 3 times a day. I believe I read that Afrin will prescribe up to 8 mg a day if the situation calls for it.

And it's also possible that fibro and MCAS are just plain not the same thing. :)
 

Who Me?

Well-Known Member
Neuroprotek has a third ingredient, forgot what but he says 2 do the work while the 3rd distracts the stomach so the others can work.

(Can't remember where I read it but it was while searching luteolin )
 

Cort

Founder of Health Rising and Phoenix Rising
Staff member
@Cort. FYI this is what I see 2nd quote on my phone. Don't want to high jack thread. I wonder if the original article had colors that didn't translate
Wow...I took the quotes out...I got that quote from a blog I did for Phoenix Rising...it did not sit well on the HR Forums (lol)
 

Cort

Founder of Health Rising and Phoenix Rising
Staff member
Don't you think maybe this says it all?

2 mg of ketotifen is probably not nearly enough. Most I've read suggests higher doses are more effective. I'm on 1 mg 3 times a day. I believe I read that Afrin will prescribe up to 8 mg a day if the situation calls for it.

And it's also possible that fibro and MCAS are just plain not the same thing. :)
This dosing thing is soooo important. I think most studies are quite conservative - particularly with supplements. I often wonder how in the world do they expect to get effects from taking a normal dose of something. It's so sad though. Ang has surely moved on...
 

Veet

Well-Known Member
I also love Royal jelly.

But wouldn't it be something if your "mild" mast cell issues were actually responsible for your more severe symptoms too (even if seemingly unrelated)?

I just found out today that mast cells can stimulate prolactin release. I've been chasing down the root cause of that mildly elevated prolactin for years now. Could it be that it was the mast cells all along?
I would not be surprised if MC turn out to be very much involved. My symptoms have included bladder urgency, blood blisters in mouth, discharge from ears.

The other ingredient in Neuroprotek is rutin I started my natural antihistamines w/ quercetin, then found rutin was better for me. I'd quit taking them when I was no longer having overt histamine symptoms. Since learning of the connection of MC to POTS, I've resumed rj and rutin. The reason I started looking into POTS, heat flushing, has dramatically reduced or disappeared since I've put these back into my mix.

This interview of 2 women by Dr. Theoharides covers some of the broad range of symptoms.

Here Theoharides talks about mast cell/histamine storms in the brain. When my mind was non-stop, with no success in calming it, I had excellent, almost immediate results w/ Neuroprotek. After intense detox efforts, I no longer needed it. It's pricey, especially w/ postage, so I've reserved it for brain storms, not for general MC issues, and am no longer using it. And here, Theoharides talks specifically about Neuroprotek. I generally avoid specialty formulations, but trusted him and his experience in pharmacology, and am very glad I did.


http://algonot.com/product/neuroprotek/
There are approximately 3,000 flavonoids. Of those, NeuroProtek® contains three:
Luteolin (> 95% Pure) is a nutrient from a class of naturally occurring molecules known as bioflavonoids. Luteolin was incorporated in this formula after published papers showed it is important in the body as a free radical scavenger.
Quercetin ( > 95% Pure)is a natural non-acidic flavanoid. The quercetin used is NeuroProtek is obtained from the saphora plant. Algonot decisively choose not to use the more common and less expensive source of fava beans.
Rutin (> 95% Pure) is a glycoside of the flavonoid Quercetin. Like quercetin, rutin is extracted from the saphora plant and is a non-acidic natural flavonoid that adds additional anti-oxidant qualities. Rutin helps liberate quercetin in the intestine, making absorption easier. Rutin has been shown to be the strongest antioxidant in studies.
Olive Kernel Extract (Oil, Unprocessed, MicroFiltered) is a natural, potent low-acidic anti-oxidant. This unique oil (a lipid) plays an important role in NeuroProtek® as it is used to increase the absorbability of flavonoids. We use only virgin olive seed oil from the island of Crete, Greece.
Why the chosen flavonoids?
Flavonoids are naturally occurring compounds frequently found in green plants and seeds. In powder form, whether taken as pills, tablets or hard capsules, all flavonoids are difficult to absorb and are extensively metabolized to inactive ingredients in the liver. In fact, less than 10% of orally ingested flavonoids are absorbed. In addition, very few flavonoids are beneficial; instead, many others such as morin show no activity, while pycnogenol is weakly active (as compared to luteolin or quercetin) but could cause liver toxicity.
As an additional consideration, the most common commercial source of the flavonoid quercetin is fava beans, which can be detrimental to blood cells in those of Mediterranean origin (15%), who lack the enzyme glucose-phosphate dehydrogenase (G6PD). Quercetin and its closely, structurally related flavonoids – rutin and luteolin, have potent anti-oxidant actions.
Can other preparations of the elect flavonoids be used?
There are about 3,000 flavonoids in nature and many impure flavonoids are sold under such names as
“bioflavonoids,” “citrus flavonoids,” “soy flavonoids,” or “pycnogenol.” Even those preparations claiming to
have only the select flavonoids, DO NOT specify either the source or the purity of the flavonoids
. This problem is even worse given that many people could have reactions to the impurities, fillers or dyes.
 

Who Me?

Well-Known Member
@Veet. I've been looking at neuroprotek since seeing the videos from the doc.

I may not have typical mast cell but i sure do wonder if something is going on in my brain.

I noticed there are 2 types of neuroprotek. One is low phenol. Do you know the difference (sorry if I've asked you) and how do you know which to get? Is it one capsule per day?

Like you I try not to get combos but there is a specific reason he has all 3 things in it.

Just saw one cap per 44 lbs. yikes.
 
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