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Part 4 antihistamine tutorial | PharmacoPhoto | YouTubeToText
YouTube Transcript: Part 4 antihistamine tutorial
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First-generation antihistamines, while effective for histamine-related conditions, possess significant anticholinergic side effects due to their unintended binding to acetylcholine receptors in both the brain and peripheral tissues. This binding can lead to serious adverse effects, including an increased risk of dementia and disruption of the parasympathetic nervous system.
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okay so hopefully we understood all of
that and we're getting now into
understanding anti- coleric effects in
the brain and in the peripheral tissue
because the anti-histamines that were
the first generation anti-histamines had
a another problem they bound fairly
strongly to the acetal choline receptor
the muscarinic receptor not the
nicotinic receptor if they bound to the
acetylcholine nicotinic re receptor we'd
be in big trouble because we'd be
winding up with muscle weakness and
things like that but no they only bind
to The muscarinic receptors we've got
muscarinic acetylcholine receptors up in
the brain and we've up muscarinic acetal
choline receptors in the parasympathetic
nervous system and this portion actually
deals with that now what I'll do is I'll
actually before I even start talking
about that too much what I'll do is copy
and paste this into the chat board and
give you an idea of what sub question so
go ahead and copy and paste that one and
we're just going to talk about uh
crossover effects of anti histamines
also the crossover effects of
medications in general now one of the
important things to realize is that our
medications one of the big reasons that
our medications have any side effects at
all is because they might cross over and
and bind to some receptor or some enzyme
or something that they're not supposed
to bind to you know the perfect
medication is going to bind to only the
thing that we want it to bind to but
unfortunately a lot of our medications
inadvertently bind to something else in
addition especially if they're in a
higher dose so basically the higher the
dose gets with a medication if it for
instance has anti-cholinergic effects
it'll have much greater anticholinergic
effects as you increase the dose so as
that dose increases those bindings will
increase as well and and that is going
to result in a lot of the side effects
of medications our medications and if
you take a look at this simplistic uh
representation of the anti-histamine
trying to bind to exactly what it wants
needs to bind to so this anti-histamine
wants to bind to the histamine one
receptor that's the only thing that it
wants to bind to that's the only thing
that it should bind to if it's going to
be the perfect medication
unfortunately with the antihistamines
and especially the ones that were the
first generation antihistamines
Unfortunately they also bound to the
acetal Coline receptor fairly strongly
now all of our antihistamines have
varying degrees of binding to the
acetylcholine receptor don't get me
wrong none of them just don't bind to
them at all but in general our first
generation antihistamines the old ones
bound much stronger to the acetyl
choline receptor and therefore had what
we call anti-cholinergic or
antimuscarinic effects so that is what
was happening with the first generation
antihistamines and this is this portion
of the tutorial is really important and
the reason that it's a three-point
question instead of a two-point question
or whatever is because of the fact that
a lot of our medications like to bind to
that acetal choline receptor and
decrease the the actual actions of
acetal choline in the parasympathetic
nervous system and also a lot of our
medications will actually get uh have
anti-colic effects and go into the
bloodb brain barrier and act on those
receptors over there so this is a very
common thing and by the end of this
portion of the tutorial you'll actually
understand why a lot of our medications
wind up with dry mouth you know why is
it that your grandmother is going to
always complain about her medications
causing dry mouth because something in
that group of medications is causing a
dry mouth it's it's it has that
anti-colic effect most likely there's
other reason there there there's other
potential reasons but that's the most likely
likely
one so uh the very first thing that we
need to do is is actually look at this
one right here which doesn't really have
to do with the adverse effects of the
acetyl choline uh binding in the brain
uh the antihistamines the first
generation antihistamines that broke
into the bloodb brain barrier and went
into to the uh the brain they actually
affected the other neurotransmitter that
goes from the vestibular area through
the vestibular portion of the vestibular
cular nerve to the vomiting Center so
there's two neurotransmitters there
there's primarily the histamine one but
there's also acetal choline uh this is a
question from the above information from
that information that we just had you
just answer on the chat board what is do
you what do you think our very best
sickness the the D Dien hydramine and
other first generation antihistamines
okay so Dien hydramine and other first
generation antihistamines just in in
just as a a summary they are going to
actually block the histamine one
receptor which goes from the vestibular
area to the vomiting Center and they're
going to block the other
neurotransmitter which is going to carry
that message that you're sick from the
motion so with respect to our very best
medications for
decreasing uh motion sickness it will be
the antihistamines so I just wanted to
point that out that there is a a good
reason for it being the most commonly
prescribed or most commonly
recommended uh medication for F
sickness the other thing about this
though and the more important thing
especially with respect to the actual
question is the fact that the acetal
choline is really important in memory in
the in the brain and to give you an
example of why it's that
important uh the medications that we
have that are currently the most
effective for reducing the symptoms of
or of um of Alzheimer's disease and
other forms of demena of dementia are
going to increase the amount of acetal
choline in the brain so therefore the
very thing that we want is an increased
level of acetylcholine in the brain and
obviously as you're taking an
anti-histamine like dyen hydramine we're
decreasing the acetylcholine levels in
the brain and the other really really
important thing that I want you to
address in this question is that any of
those medications including the first generation
generation
antihistamines any of those medications
that actually bind to the acetylcholine
receptor and block it and they're in the
brain blocking the acetylcholine
receptor they're going to increase the
risk of developing Alzheimer's disease
and other forms of dementia so really
you shouldn't really be taking it for
long periods of time like Mrs Myers is
taking it at all especially at her age
because she already has and and as a
matter of fact you would say it is
contraindicated for Mrs Mars or you know
in a person of advancing age so a person
of advancing age has that risk of
developing Alzheimer's disease if you
have another risk factor like you know
taking antihistamines every single day
that's going to be another if you have
another risk factor like familial
predisposition that's going to to be
another uh kind of risk factor so uh it
it it's really important for this client
especially it's really important that
she gets off of the antihistamines now
and uh just allows as much acetal
choline there as possible so that's
what's happening in the brain and that's
relevant by the way just it's relevant
to any of our medications that
inadvertently uh kind of bind to the
acetylcholine the muscarinic
acetylcholine receptor that break into
the bloodb brain barrier actually kind
of seriously increasing the risk of
developing Alzheimer's at the same
time so uh the peripheral
anti-cholinergic effects of medications
you know like we will see this really
quite frequently we know that it's going
to be seen and the best way to really
kind of um kind of picture it is with a
picture like this where you got the
parasympathetic nervous system over here
and the sympathetic nervous system over
here and remember that that's one of our
ways of having homeostasis how do we
actually control the internal
environment and regulate it and make
sure that it's balanced well we've got
the Sy one of the ways is the
sympathetic and the parasympathetic
nervous system and virtually they do the
opposite kind of effect so anytime
you're blocking one of these if it has a
general an
antimuscarinic effect all the way
through the body what you're doing is
blocking this side over here the
parasympathetic nervous system and
allowing the sympathetic nervous system
to dominate so really easy on this one
you can actually think about you know
what happens in the pupils of the eyes
when you're just resting and relaxing
and there's no lights on and you're just
kind of really relaxing and just about
ready to go to sleep uh you know you've
you've got the lights dimmed it's going
to be a constriction of the pupils but
then if you're going to be eliminating
or decreasing the actions of the
parasympathetic nervous system then
what's going to happen is the the pupils
will dilate that's going to possibly
give a person a little bit of blurred
vision and it's also going to possibly
give the person a little bit of eye pain
because they might be a little bit too
bright a light so those are some of the
that's one couple of the uh primary
things that you find with an
anti-colic uh drug another thing that
happens with the parasympathetic nervous
system it's the rest and digest system
so we're resting and digesting but the
entire digestive system is going to be
going over time and just stimulated and
that kind of thing so therefore you know
you're going to have lots of saliva for
instance in the parasympathetic nervous
system kind of actions but then if you
cross that out if you actually uh bind
to those receptors those muscarinic
receptors and allow the sympathetic
nervous system to dominate then what
happens you've got an in inhibition of
salivation one of the things that
happens with a really severe like if
people in battle for instance we'll
actually talk about this uh the mouth
becomes so dry a very very dry mouth as
you have that severe sympathetic nervous
system stimulation and almost impossible
to uh to swallow but what you're ending
up to do on with with this you're
allowing that sympathetic nervous system
to dominate inhib inhibiting the
salivation and having a dry mouth now
it's got a lot of other effects as well
but the main effects the other main
effect that the person will be having is
going to be the the fact that the
sympathetic nervous system is the we
need to flee not we we've got to get out
of there and not take the time to uh you
know to urinate you know we've got to
get out of there so that's the other
thing that a person who is on a
anti-colic drug they're going to wind up
with not being able to urinate as well
so you can mention in in the answer to
this question you can mention some of
the other ones certainly mentioned some
of the other anti- coleric effects that
you find I'm going to allow you to
research this one a little bit more I'm
not going to give you every single
portion of the answer to this one you do
a little bit of work it's the most
important one and that's why I want you
to do a little bit of research you know
what are the anti-colic effects of a
first generation anti-histamine for
instance that might be a good search and
you'll find urinary retention because we
need def Fleet not we were're allowing
the sympathetic nervous system to
dominate uh dry mouth and other git
complaints because of the fact that
you're shutting down the rest and digest
system um and basically what you'll be
uh explaining is Dien hydramine is going
to cause is going to do a couple things
um with its binding to the acetylcholine
receptor as it binds to the
acetylcholine receptor in the brain
it's going to result in this as it binds
to the acetylcholine receptor on our
organs on our internal organs it's going
to do these things as well so just talk
about it in that way and it is a very
important thing so just make sure you
spend a little bit extra time on that
what I'm going to do right now is look
at and then how do you treat dry mouth
um you can stop taking the the drug
that's causing the dry mouth which often
times has to happen because some some
people don't get relief there are lenes
and that kind of thing that try to
stimulate the the saliva and uh try to
have the person tolerate the medication
a lot of people just simply from the dry
mouth they actually have to get off of
the medication that has the anti-colic
effects so were there any other
questions on this before we sign out one
thing that we don't ever do in this unit
is just grab 100 different side effects
of a medication and just stick it into
our workbook or whatever we whatever it
happens to be we we just don't do that
we don't kind of stick all of those side
effects we have to find out what the
most important side effects are what the
ones that actually are most frequently
uh found and also the ones that are most
most profound you know so for instance
the fact that this medication actually
causes an increased risk of developing
Alzheimer's disease that's really
important so uh so you really do put
down that kind of thing and you
definitely put down the things that I
talked about with respect to the
peripheral anti-cholinergic effects
because those are all really important
as well but like I said you might add to
those okay guys thanks for all the
things for coming in and I I do um kind
of uh look forward to seeing you next
week if you decide to come here next
week and if not then you can hit the uh
video tutorial series you can test out
that video tutorial series when it goes online
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