Jump to content
Construct

What supplements do you take regularly? 2019 Edition.

Recommended Posts

This anti-histamine discussion is all very interesting. I never noticed any sedation from cetirizine, but I always felt that it worked better than loratadine, especially when my symptoms are stronger in the spring. I do have a tendency to be irritable midday, but I always thought that was from the caffeine, not the cetirizine. Worth trying it at night to see if it makes a difference.

 

This discussion does make me interested in re-exploring the various options for non-BBB penetrating second-gen anti-histamines, though.

Share this post


Link to post
Share on other sites

I found this, which was an interesting summary: "At higher-than-recommended doses, sedation can occur with loratadine.4 Some patients taking cetirizine may experience sedation even at recommended doses.6 Fexofenadine, even at higher-than-recommended doses, has not been associated with sedation.7,15"

 

So it sounds like I chose the most drowsy of the three and should probably try fexofenadine and loratadine again.

Share this post


Link to post
Share on other sites
4 minutes ago, Mr.Kite said:

I found this, which was an interesting summary: "At higher-than-recommended doses, sedation can occur with loratadine.4 Some patients taking cetirizine may experience sedation even at recommended doses.6 Fexofenadine, even at higher-than-recommended doses, has not been associated with sedation.7,15"

 

So it sounds like I chose the most drowsy of the three and should probably try fexofenadine and loratadine again.

That data was the inspiration for my Fexofenadine trial. I remember being disappointed because my results were the exact opposite of what I expected.

 

Before my allergies mysteriously disappeared a few years ago, I was taking a double dose of Loratidine every day during spring and summer without any issues. Fortunately for all of us, these are now inexpensive and available over-the-counter, so experimentation is easy enough.

Share this post


Link to post
Share on other sites

If we are really looking at the best OTC available with the least peripherals, I am guessing it would probably be bilastine at this point in time.

Share this post


Link to post
Share on other sites
22 minutes ago, Ras said:

If we are really looking at the best OTC available with the least peripherals, I am guessing it would probably be bilastine at this point in time.

 

That is an interesting one. It looks like it is just as potent as cetirizine, but with fewer side effects. I'll have to try it once I get to Germany since it is EU only for the time being.

Share this post


Link to post
Share on other sites

My recollection is that cetirizine sedation in certain individuals stems from genetic MDR1/P-gp polymorphisms leading to increased CNS distribution in those with the hypofunctional transporter genotype(s).  

 

I don't know about the irritability from this or other antihistamines in terms of mechanism, other than that I believe its real as I have a friend that gets very irritable and anxious from even acute use of diphenhydramine.  

 

Somewhat paradoxically, hydroxyzine (which is prob. my fav antihistamine in general btw, if it weren't for the dangers of chronic use, which are serious) seems to have anxiolytic effects from my experience (off-target mechanisms?).

Share this post


Link to post
Share on other sites

I've always associated, possibly mistakenly, diphen irritability with anticholinergic shit. Thinking slowly makes me fucking mad.

Share this post


Link to post
Share on other sites
17 minutes ago, nightop said:

Somewhat paradoxically, hydroxyzine (which is prob. my fav antihistamine in general btw, if it weren't for the dangers of chronic use, which are serious) seems to have anxiolytic effects from my experience (off-target mechanisms?).

 

Hydroxyzine antagonizes the 5-HT2A receptor like trazodone and also one of the dopamine receptors which probably contribute to its anxiolytic effects.

 

As far as risks, are you referring to QT interval changes?

Share this post


Link to post
Share on other sites

I've been using Xyzal, which apparently is a 3rd generation antihistamine related to Zyrtec. Seems to be less sedating, but it could just be my imagination. I take it at night.

Share this post


Link to post
Share on other sites

I'm a dinosaur, I still take benadryl. I take cetirizine when I am experiencing long-term (1+ weeks) hayfever and I'm going to take it daily, but largely I take benadryl when I'm miserable and need reliefe ASAP.

Share this post


Link to post
Share on other sites
8 minutes ago, Kimbo said:

I've been using Xyzal, which apparently is a 3rd generation antihistamine related to Zyrtec. Seems to be less sedating, but it could just be my imagination. I take it at night.

 

It is literally the same thing as Zyrtec. Zyrtec is a racemic mixture of citirizine at 10mg, while Xyzal is a 5mg dose of the L-isomer. Unless there is evidence showing that the D-isomer in Zyrtec is the cause of sedation, I can't see the benefit.

Share this post


Link to post
Share on other sites

It's just the L-enantiomer and my sense was that was a marketing decision rather than a pharmacological decision...they roll those out when the patent on the original molecule runs out....see also desloratadine.

Share this post


Link to post
Share on other sites

There's a lot to be said for enantiomer specificity in certain cases. I have no idea if that is the case here or not.

Share this post


Link to post
Share on other sites
1 hour ago, Ras said:

There's a lot to be said for enantiomer specificity in certain cases. I have no idea if that is the case here or not.

 

True that. D-amphetamine is a DEA controlled substance and L-amphetamine is available OTC.

Share this post


Link to post
Share on other sites

There is zero doubt that they do that shit for patent evergreening as well, just like emergent indications that magically appear at the end of a patent cycle.

Share this post


Link to post
Share on other sites
2 hours ago, STENDEC said:

 

Hydroxyzine antagonizes the 5-HT2A receptor like trazodone and also one of the dopamine receptors which probably contribute to its anxiolytic effects.

 

As far as risks, are you referring to QT interval changes?

Interesting, didn't know that but it makes sense.  And no, I was referring actually to the neurotoxic/degenerative effects on DA neurons related to motor control, if I'm remembering correctly. 

 

EDIT:  I found the ref I was thinking of and it's actually more specifically tardive dyskinesia -- seems to emerge after 6+ months of chronic use.. I can't access the fulltext right now but I can tomorrow if anyone is curious.

Share this post


Link to post
Share on other sites

It's pretty widely used off label for anxiety and insomnia so I am curious what the incidence of tardive dyskinesia is with chronic use.

 

I've used it occasionally for insomnia but it has a really long half-life so it leaves me sort of foggy the next day.

Share this post


Link to post
Share on other sites
54 minutes ago, nightop said:

Interesting, didn't know that but it makes sense.  And no, I was referring actually to the neurotoxic/degenerative effects on DA neurons related to motor control, if I'm remembering correctly. 

 

EDIT:  I found the ref I was thinking of and it's actually more specifically tardive dyskinesia -- seems to emerge after 6+ months of chronic use.. I can't access the fulltext right now but I can tomorrow if anyone is curious.

 

This might be one of those things that's changed since you went astray...

 

www.sci-hub.tw

 

All FT, all the time...

Share this post


Link to post
Share on other sites
30 minutes ago, STENDEC said:

It's pretty widely used off label for anxiety and insomnia so I am curious what the incidence of tardive dyskinesia is with chronic use.

 

 

Hydroxyzine is selective for H1 at low enough doses. The D2 and 5-HT2A action require higher doses. I'm not sure what doses are common for insomnia but it's possible that the D2 action just isn't significant for low-dose insomnia treatment.

 

I'm interested in trying a selective H1 antagonist for insomnia, but it's difficult to find a selective H1 antagonist with the right half-life to avoid next-day grogginess. Doxepin might come closest.

 

Alternatively, I might try very low doses of Trazodone to test the 5-HT2A selectivity for insomnia. Trazodone has such a high affinity for 5-HT2A that 1mg is thought to be sufficient to occupy 50% of 5-HT2A receptors in humans. That's just 2% of the smallest available Trazodone pill formulation. At the common 50mg dose, alpha-1, SERT, and H1 are all in play.

Share this post


Link to post
Share on other sites

Create an account or sign in to comment

You need to be a member in order to leave a comment

Create an account

Sign up for a new account in our community. It's easy!

Register a new account

Sign in

Already have an account? Sign in here.

Sign In Now

×
×
  • Create New...