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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 5 of 5. This is the beginning of the thread.
Posted by Betternow on January 29, 2004, at 0:10:43
antagonize 5ht2a, agonize 5ht1a, it could have some reuptake inhibition-5ht and/or NE. IT MUST NOT effect alpha1 adrenergic receptors, the cholinergic muscarinic receptors, or the histamine H1 receptors.Geodon is close but its alpha1 antagonism kills it for me. I cannot do alpha blockers, they make me a stupid zobie with a bad case of sinusitus.
In the abscence of such aperfect drug, Anyone have any ideas on counteracting the Alpha1 adrenergic antaganism present in drugs like serzone, geodon, trazadone, mirtazapine, etc. It is that property of these drugs that make us feel like crap.
Has anyone got an idea on how to counteract. Could one take an Alpha1 adrenergic AGONIST to offset?
Sick and tired of the SSRIs-gotta find alternative
Not so Betternow
Posted by scott-d-o on January 29, 2004, at 0:50:55
In reply to I NEED A DESIGNER DRUG ASAP!!!!!! It will........., posted by Betternow on January 29, 2004, at 0:10:43
> antagonize 5ht2a, agonize 5ht1a, it could have some reuptake inhibition-5ht and/or NE. IT MUST NOT effect alpha1 adrenergic receptors, the cholinergic muscarinic receptors, or the histamine H1 receptors.Geodon is close but its alpha1 antagonism kills it for me. I cannot do alpha blockers, they make me a stupid zobie with a bad case of sinusitus.
>
> In the abscence of such aperfect drug, Anyone have any ideas on counteracting the Alpha1 adrenergic antaganism present in drugs like serzone, geodon, trazadone, mirtazapine, etc. It is that property of these drugs that make us feel like crap.
>
> Has anyone got an idea on how to counteract. Could one take an Alpha1 adrenergic AGONIST to offset?
>
> Sick and tired of the SSRIs-gotta find alternative
>
> Not so Betternow
>
here u go:http://www.biopsychiatry.com/flibanserin.html
no reuptake inhibition... but one med can't do everything, can it?
Posted by Questionmark on January 29, 2004, at 15:08:15
In reply to I NEED A DESIGNER DRUG ASAP!!!!!! It will........., posted by Betternow on January 29, 2004, at 0:10:43
> antagonize 5ht2a, agonize 5ht1a, it could have some reuptake inhibition-5ht and/or NE. IT MUST NOT effect alpha1 adrenergic receptors, the cholinergic muscarinic receptors, or the histamine H1 receptors.Geodon is close but its alpha1 antagonism kills it for me. I cannot do alpha blockers, they make me a stupid zobie with a bad case of sinusitus.
>
> In the abscence of such aperfect drug, Anyone have any ideas on counteracting the Alpha1 adrenergic antaganism present in drugs like serzone, geodon, trazadone, mirtazapine, etc. It is that property of these drugs that make us feel like crap.i understand how that alpha1 adrenergic antagonism would be a pain i think. But alpha2 antagonism shouldn't be a bad thing, unless it is too severe or you are extremely susceptible to panic or anxiety. And i'm not sure about Serzone or Geodon, but i know that trazadone's and mirtazapine's adrenergic effects are antagonism of alpha2 receptors. This increases release of NE and, to some extent, 5-HT, and it is good for sexual functioning, esp. that of males. i believe this is actually why one of trazadone's potential dangerous side effects is priapism (b/cz of its alpha-2 antagonism).
> Has anyone got an idea on how to counteract. Could one take an Alpha1 adrenergic AGONIST to offset?
>
> Sick and tired of the SSRIs-gotta find alternative
>
> Not so Betternow
Posted by Betternow on January 29, 2004, at 19:40:05
In reply to Re: ...Designer.... It will......... » Betternow, posted by Questionmark on January 29, 2004, at 15:08:15
>
> i understand how that alpha1 adrenergic antagonism would be a pain i think. But alpha2 antagonism shouldn't be a bad thing, unless it is too severe or you are extremely susceptible to panic or anxiety. And i'm not sure about Serzone or Geodon, but i know that trazadone's and mirtazapine's adrenergic effects are antagonism of alpha2 receptors. This increases release of NE and, to some extent, 5-HT, and it is good for sexual functioning, esp. that of males. i believe this is actually why one of trazadone's potential dangerous side effects is priapism (b/cz of its alpha-2 antagonism).
>Hi ?
I really appreciate your response!
I'm not even close to being smart about this stuff, but based on clinical pharmacology from product information, you are correct about Mirtazapine's therapeutic benefits from antagonism of alpha2 autoreceptor. This is a good thing! I guess.
But it also says it antagonizes alpha1 and this may be responsible for orthostatic hypotension-not so good!
If anybody out there is really up on this stuff, I would appreciate something like "Receptors for Dummies"
I don't know the difference between a "receptor", an "autoreceptor" or certainly a "heteroreceptor".
Posted by Questionmark on January 30, 2004, at 16:05:00
In reply to Re: ...Designer.... It will........., posted by Betternow on January 29, 2004, at 19:40:05
> >
> > i understand how that alpha1 adrenergic antagonism would be a pain i think. But alpha2 antagonism shouldn't be a bad thing, unless it is too severe or you are extremely susceptible to panic or anxiety. And i'm not sure about Serzone or Geodon, but i know that trazadone's and mirtazapine's adrenergic effects are antagonism of alpha2 receptors. This increases release of NE and, to some extent, 5-HT, and it is good for sexual functioning, esp. that of males. i believe this is actually why one of trazadone's potential dangerous side effects is priapism (b/cz of its alpha-2 antagonism).
> >
>
>
>
> Hi ?
>
> I really appreciate your response!
>
> I'm not even close to being smart about this stuff, but based on clinical pharmacology from product information, you are correct about Mirtazapine's therapeutic benefits from antagonism of alpha2 autoreceptor. This is a good thing! I guess.
>
> But it also says it antagonizes alpha1 and this may be responsible for orthostatic hypotension-not so good!Oh really? It does? Shoot, i'm sorry. i didn't know that. That does kinda suck. Hopefully that's mild alpha1 antagonism maybe?
>
> If anybody out there is really up on this stuff, I would appreciate something like "Receptors for Dummies"
>
> I don't know the difference between a "receptor", an "autoreceptor" or certainly a "heteroreceptor".An autoreceptor is a receptor that is located on the axon (neurotransmitter-releasing end of a neuron) of a presynaptic neuron (the sending cell between a sending neuron and receiving neuron). Autoreceptors are "activated" by the neurotransmitters (NTs) that are released by that neuron (the presynaptic). When activated, they signal that neuron to DEcrease the amount of neurotransmitter released. Agonism of them by a drug therefore does the same. Antagonism of autoreceptors, then, INcreases the amount of NT released by that cell.
Heteroreceptors are exactly the same except they are activated by different NTs than those that are released by the neuron they are located on.
This is the end of the thread.
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