Psycho-Babble Medication Thread 367673

Shown: posts 1 to 13 of 13. This is the beginning of the thread.

 

Histamine H1 - Drugs to increase activity?

Posted by SLS on July 19, 2004, at 7:24:39

Hi.

I am interested in how histaminergic pathways might be involved in depression and bipolar disorder. Are there any drugs that act as H1 receptor agonists or otherwise promote histaminergic neurotransmission? Do such things exist?


- Scott

 

Re: Histamine H1 - Drugs to increase activity? SLS

Posted by Larry Hoover on July 19, 2004, at 9:59:05

In reply to Histamine H1 - Drugs to increase activity?, posted by SLS on July 19, 2004, at 7:24:39

> Hi.
>
> I am interested in how histaminergic pathways might be involved in depression and bipolar disorder. Are there any drugs that act as H1 receptor agonists or otherwise promote histaminergic neurotransmission? Do such things exist?
>
>
> - Scott

Yes, H1 histamine agonists are known. One of the central roles of histamine in the brain is as a participant in the diurnal wake/sleep cycle. For an H1 agonist drug to be useful, IMHO, its uptake and clearance time must also be in accord with the oscillations in e.g. melatonin, HGH, cortisol release which accompany movement through this cycle. Histamine does other things, too. Just what aspect of histamine function would you be trying to tweek?

Lar

 

Re: Histamine H1 - Drugs to increase activity?

Posted by SLS on July 19, 2004, at 13:44:26

In reply to Re: Histamine H1 - Drugs to increase activity? SLS, posted by Larry Hoover on July 19, 2004, at 9:59:05

> > I am interested in how histaminergic pathways might be involved in depression and bipolar disorder. Are there any drugs that act as H1 receptor agonists or otherwise promote histaminergic neurotransmission? Do such things exist?

> Yes, H1 histamine agonists are known. One of the central roles of histamine in the brain is as a participant in the diurnal wake/sleep cycle. For an H1 agonist drug to be useful, IMHO, its uptake and clearance time must also be in accord with the oscillations in e.g. melatonin, HGH, cortisol release which accompany movement through this cycle. Histamine does other things, too. Just what aspect of histamine function would you be trying to tweek?

I really don't know yet. I am just starting to look into it. Right now, the best I can do is to skim a few paragraphs here and there. I can't remember the last time I was able to read word for word three consecutive paragraphs. I am becoming interested in the DLPFC (dorsolateral prefrontal cortex) as being the site most affected in my case. Some of the afferent circuits are histaminergic. I am curious if any pro-histaminergic drugs have been screened for depression.


- Scott

 

Exposing my utter ignorance here, but... SLS

Posted by Racer on July 19, 2004, at 16:47:32

In reply to Re: Histamine H1 - Drugs to increase activity?, posted by SLS on July 19, 2004, at 13:44:26

Truly, I am totally ignorant in this, but I do have a little bit of anecdotal trivia to throw in on this one:

One of the symptoms of Cushing's syndrome is depression, and one of the treatments studied for Cushing's used periactin alone. There's conflicting evidence for efficacy, but a lot of support for trying it as a first line treatment due to the low cost. SLS, this isn't something I want to throw out in public -- sorry, long story, trigger subject for me -- but if you want to drop me an email I'll offer up what I do know on the subject. Basically, though, I've seen it help a heck of a lot, so you're probably onto something and it just might be helpful for you. I wish you the best, always, and hope that you do find something good. Let us know your results, of course.

My best wishes to you.

 

Re: Exposing my utter ignorance here, but... Racer

Posted by Larry Hoover on July 20, 2004, at 9:40:08

In reply to Exposing my utter ignorance here, but... SLS, posted by Racer on July 19, 2004, at 16:47:32

> Truly, I am totally ignorant in this, but I do have a little bit of anecdotal trivia to throw in on this one:
>
> One of the symptoms of Cushing's syndrome is depression, and one of the treatments studied for Cushing's used periactin alone. There's conflicting evidence for efficacy, but a lot of support for trying it as a first line treatment due to the low cost. SLS, this isn't something I want to throw out in public -- sorry, long story, trigger subject for me -- but if you want to drop me an email I'll offer up what I do know on the subject. Basically, though, I've seen it help a heck of a lot, so you're probably onto something and it just might be helpful for you. I wish you the best, always, and hope that you do find something good. Let us know your results, of course.
>
> My best wishes to you.

Cyproheptadine (Periactin) is antiseritonergic, according to the drug monograph. I'm sorry you don't feel comfortable talking about it here, but you have certainly raised my curiosity.

Lar

 

Re: Histamine H1 - Drugs to increase activity? SLS

Posted by Larry Hoover on July 20, 2004, at 9:47:31

In reply to Re: Histamine H1 - Drugs to increase activity?, posted by SLS on July 19, 2004, at 13:44:26

> I really don't know yet. I am just starting to look into it. Right now, the best I can do is to skim a few paragraphs here and there. I can't remember the last time I was able to read word for word three consecutive paragraphs. I am becoming interested in the DLPFC (dorsolateral prefrontal cortex) as being the site most affected in my case. Some of the afferent circuits are histaminergic. I am curious if any pro-histaminergic drugs have been screened for depression.
>
>
> - Scott

Well, pace yourself. Don't push yourself to exhaustion. It isn't worth it. What you can do is what you can do.

There are a number of antidepressants which have been found to coincidentally hit H1 receptors: Remeron, doxepin, trimipramine, amitryptiline. I don't know about pure H1 activity, off the top of my head. There are anecdotal reports that some of the modern antihistamines have some selective H1 activity, notwithstanding their advertised "non-drowsy" status, but I can't remember which one (or ones). Benadryl (diphenhydramine) is a non-specific histaminic, but tolerance often very quickly develops to it. If you try a dose of Benadryl just before retiring for the night, and you awake feel more restored by sleep, maybe that will be the sort of clue you're looking for?

Lar

 

Re: Exposing my utter ignorance here, but... Larry Hoover

Posted by Racer on July 20, 2004, at 12:00:45

In reply to Re: Exposing my utter ignorance here, but... Racer, posted by Larry Hoover on July 20, 2004, at 9:40:08

>
> Cyproheptadine (Periactin) is antiseritonergic, according to the drug monograph. I'm sorry you don't feel comfortable talking about it here, but you have certainly raised my curiosity.
>
> Lar
>
>
If you're interested -- and aren't expecting much -- you can email me and I will try to respond in a timely manner. babbler39 at excite dot com. The last few days have just left me wiped out, emotionally, although I can't quite tell why. Just very, very low. I don't have a whole lot of really great info, but what I do know you're welcome to. Just not at all something I want to have in public, you know?

 

Re: Histamine H1 - Drugs to increase activity?

Posted by TenMan on July 20, 2004, at 12:12:47

In reply to Re: Histamine H1 - Drugs to increase activity? SLS, posted by Larry Hoover on July 20, 2004, at 9:47:31

Wait, I'm a little confused. Scott, are you looking for an anti-histamine or a histamine agonist?

 

Re: Histamine H1 - Drugs to increase activity? TenMan

Posted by Larry Hoover on July 20, 2004, at 14:14:32

In reply to Re: Histamine H1 - Drugs to increase activity?, posted by TenMan on July 20, 2004, at 12:12:47

> Wait, I'm a little confused. Scott, are you looking for an anti-histamine or a histamine agonist?

Doh! If there's any confusion, it's probably been introduced by me. Sorry. I feel a wee bit stunned today.

Lar

 

Re: Histamine H1 - Drugs to increase activity? SLS

Posted by Cairo on July 21, 2004, at 9:13:12

In reply to Histamine H1 - Drugs to increase activity?, posted by SLS on July 19, 2004, at 7:24:39

http://www.biopsychiatry.com/histamine.htm
http://www.biopsychiatry.com/antideps/

Biopsychiatry and HedWeb are great sources of info.

Cairo

 

Re: Histamine H1 - Drugs to increase activity? SLS

Posted by Questionmark on July 22, 2004, at 4:58:25

In reply to Histamine H1 - Drugs to increase activity?, posted by SLS on July 19, 2004, at 7:24:39

> Hi.
>
> I am interested in how histaminergic pathways might be involved in depression and bipolar disorder. Are there any drugs that act as H1 receptor agonists or otherwise promote histaminergic neurotransmission? Do such things exist?
>
>
> - Scott


Very novel and interesting thought, Scott. i've been curious as to what a histamine agonist might be like for awhile as well, though maybe not to the extent that you have. It would be very interesting to try one though, if one were available. Unfortunately, i have never heard of one, selective or not.
Take care.

 

Re: Histamine H1 - Drugs to increase activity? Questionmark

Posted by Larry Hoover on July 22, 2004, at 6:17:48

In reply to Re: Histamine H1 - Drugs to increase activity? SLS, posted by Questionmark on July 22, 2004, at 4:58:25

> > Hi.
> >
> > I am interested in how histaminergic pathways might be involved in depression and bipolar disorder. Are there any drugs that act as H1 receptor agonists or otherwise promote histaminergic neurotransmission? Do such things exist?
> >
> >
> > - Scott
>
>
> Very novel and interesting thought, Scott. i've been curious as to what a histamine agonist might be like for awhile as well, though maybe not to the extent that you have. It would be very interesting to try one though, if one were available. Unfortunately, i have never heard of one, selective or not.
> Take care.

Sorry for any confusion I may have added to this thread, but my brain has been misfiring lately, apparently due to Zoloft. In some instances, I was reading affinity, but thinking agonism.

However, there is a potent H1 agonist, 8R-lisuride. There are also some histamine analogs with higher agonistic potential than histamine itself.

Perhaps more useful, though, from a pharmacological standpoint, are drugs which agonize or antagonize the H3 histamine synaptic autoreceptor. It directly regulates histamine synthesis and release in the brain. I believe there are H3 drugs entering the clinical trial arena round about now.

Lar

 

Re: Histamine H1 - Drugs to increase activity?

Posted by SLS on July 22, 2004, at 8:44:07

In reply to Re: Histamine H1 - Drugs to increase activity? Questionmark, posted by Larry Hoover on July 22, 2004, at 6:17:48


> Perhaps more useful, though, from a pharmacological standpoint, are drugs which agonize or antagonize the H3 histamine synaptic autoreceptor. It directly regulates histamine synthesis and release in the brain. I believe there are H3 drugs entering the clinical trial arena round about now.

Now, that sounds encouraging. Thanks, Larry.


- Scott


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