Last summer, I wrote a lot about autism getting much worse
in that time of the year and how I found that common “24 hour” anti-histamine
drugs seemed to have a magical effect; but one that lasted only 2-3 hours.
There were only visible signs of a mild allergy, which could indeed easily be
overlooked.
I did later receive a message from a reader who noticed his
child’s ASD behaviours were greatly improved by Zrtec and his doctor agreed to
prescribe this H1 antihistamine all year round.
Recently, I stumbled upon a blog, rich with many comments
of parents of kids with severer types of autism. Here I noted some parents referring to “summertime
raging”, and I thought to myself, I know what they mean. Fortunately, I found out how to make it go
away.
Ant-histamine
drugs
The two most common antihistamine drugs are Claritin
(Loratadine), its active derivative Aerius (Desloratadine) and Zrtec (Ceterizine) and its
active derivative Xyzal (levocetirizine).
The main
action of an antihistamine is not actually to reduce the amount of histamine in
your blood, rather it is to block the effect of histamine on the H1 receptors.
An H2
antihistamine blocks H2 receptors that are mainly in your intestines, and is
used to reduce the amount of acid in the stomach.
This led me
on a quest for substances that actually stop the increase in histamine, rather
than just blocking some effects. The
only thing that does this is something that can stop so-called mast cells from
degranulating and spilling their load of histamine, serotonin, nerve growth
factor and cytokines, including IL-6, into the blood; from where, all except
serotonin, are free to travel to the brain, across the blood brain barrier
(BBB). Serotonin cannot cross the BBB.
According to
the mast cell specialist Theoharides, conventional drugs are not genuine mast
cell stabilizers. There are some partial
ones, like Ketotifen, Cromalin, Rupatadine and Azelastine, but Theoharides thinks
naturally occurring flavonoids like Luteolin and Quercetin work best.
Last summer in this blog I looked at newly discovered histamine receptors types H3 and H4 which are
known to be present in the brain.
So how is it
that Claritin and Zrtec can reduce autistic behaviours ?
I did note that
both the above drugs did reduce summertime raging and also the Theoharides' research
that showed they probably should not, since they are not mast cell
stabilizers.
Since my
blog reader also found Zrtec helpful, so much so he gives it to his kid year
round and it now seems summertime raging is not an unusual phenomenon in
autism, I did some more checking.
In spite of
what Theoharides tells us, it turns out that both Claritin and Zrtec do indeed
reduce the amount of histamine in the blood.
Also, it
turns out that not only is the pro-inflammatory cytokine IL-6 released from
mast cells but it is also released from another type of cell, called the endothelial cell.
The endothelium is the thin layer of cells
that lines the interior surface of blood vessels and lymphatic vessels, forming
an interface between circulating blood or lymph in the lumen and the rest of
the vessel wall. The cells that form the endothelium are called endothelial cells. Endothelial cells
in direct contact with blood are called vascular endothelial cells, whereas
those in direct contact with lymph are known as lymphatic endothelial cells.
And what
prompts endothelial cells to release IL-6? Histamine does.
Indeed we
have studies showing how Claritin (loratadine) and Zrtec (Ceterizine) reduce histamine
and IL-6; it is the IL-6 from the endothelial cells.
"CONCLUSION:
These results demonstrate that both L and DCL
are active to reduce the histamine-induced activation of EC. Interestingly, DCL
seems to be effective at lesser concentrations especially to inhibit cytokine
secretion."
The above
study would suggest that Aerius (DCL) should be more effective than Claritin
(L) its predecessor.
"Histamine is a
major constituent of the mast cell. The effect of histamine on endothelial
cells is primarily mediated through H1R
Collectively,
our results suggest that mast cell-derived histamine and proteases play an
important role in vascular inflammation and calcification in addition to their
well-recognized participation in allergic diseases."
This study, and others like it, show how mast
cell degranulation contributes to heart disease. This would suggest that mast cell stabilizers
have a much wider role in human health than is realized. Another example of how a red apple a day
(with the skin) may indeed help keep the doctor away and a glass of red wine will do
the same. Both are rich sources of the
mast stabilizer Quercetin. The alcohol
increases the bio-availability.
"Conclusion
These results suggest that cetirizine exerts its
beneficial effects on viral myocarditis by suppressing expression of
pro-inflammatory cytokines, genes related to cardiac remodeling in the hearts
of mice."
So how do
Claritin and Zrtec reduce summertime/year round raging in autism? Well it could be histamine or it could be
IL-6, we cannot know for sure. The
science tells us that the brain has many H3 and H4 receptors, so they are possibly
to be implicated. Or, it may just be
IL-6; histamine’s involvement could be
just provoking the endothelial cells to release more IL-6.
Conclusion
Claritin/Zrtec/Xyzal
are relatively cheap, in theory they are long lasting drugs. In Monty, aged 10 with ASD, they all work for
summertime time raging, but not for long.
Adults should take one per 24 hours.
Monty would need one every 3 hours.
The,
supposedly better, mast cell stabilizers like Ketotifen and Rupatadine take a few
days before they have any effect at all.
Azelastin is available as a nasal spray and is supposed to be effective quickly
as an allergy treatment.
My preferred
mast cell stabilizing, IL-6 inhibiting, strategy is to combine PEA (palmitoylethanolamide)
which is already naturally in your body, with the flavonoid quercetin, which is
found in the skin of red apples and red grapes.
In theory, according to the research, this is both a potent combination
and should be free of harmful side effects.
Very frequent doses of Claritin/Zrtec/Xyzal are not going to be good.
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