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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 20 of 20. This is the beginning of the thread.
Posted by linkadge on January 13, 2005, at 14:23:43
Does anyone know what the most selective 2a blocker that we have available.
Is it remeron, or one of the TCA's ??
Linkadge
Posted by tensor on January 13, 2005, at 14:46:30
In reply to what is most selective 2a blocker we have ??, posted by linkadge on January 13, 2005, at 14:23:43
Hi Link,
cyproheptadine is a strong 2a antagonist, it's also indicated for AD sexual side effects. I think it's pretty selective, though i've never tried it.
/Mattias
Posted by Larry Hoover on January 13, 2005, at 15:01:24
In reply to what is most selective 2a blocker we have ??, posted by linkadge on January 13, 2005, at 14:23:43
> Does anyone know what the most selective 2a blocker that we have available.
>
> Is it remeron, or one of the TCA's ??
>
>
> LinkadgeI'm not sure what you're meaning by "most selective". Risperidone and ziprasidone are probably the most potent common medications.
The thing is, there are always other receptors that are hit by the drug you might select, which is why I wonder what you're after with "selective".
Just put 5-HT2a in the "Receptor name" box, and submit.
If you wonder what else a particular drug affects, go back to the query page, and enter the drug name under "Test ligand", and clear the receptor box.
Lar
Posted by King Vultan on January 13, 2005, at 15:02:31
In reply to what is most selective 2a blocker we have ??, posted by linkadge on January 13, 2005, at 14:23:43
> Does anyone know what the most selective 2a blocker that we have available.
>
> Is it remeron, or one of the TCA's ??
>
>
> Linkadge
Risperdal at dosages of less than 1 mg/day is easily the most selective 5-HT2A blocker among psychotropic drugs. Remeron's H1 blockade is about 10 times stronger than its 5-HT2A blockade, and Remeron's 2A blockade is only a little more selective than its 2C blockade (Ki of 1.48 vs. 4.1, respectively).In contrast, Risperdal's 5-HT2A blockade is probably about 20 times stronger than its next relevant blockade (alpha-1 adrenergic). It is also extremely selective for the 2A vs. 2C receptor (Ki of 0.15 vs. 32, a factor of about 200x). Geodon would be the closest to Risperdal in terms of overall selectivity for the 2A receptor, but it is not particularly selective for the 2A vs. 2C receptor.
Todd
Posted by linkadge on January 13, 2005, at 16:48:07
In reply to Re: what is most selective 2a blocker we have ?? » linkadge, posted by King Vultan on January 13, 2005, at 15:02:31
I just want something to augment my zoloft without it having too much extra effect.
I know selective is a relative term but, some have more affinity for the 2a receptors than other systems they affect.Linkadge
Posted by Larry Hoover on January 13, 2005, at 17:45:13
In reply to Re: what is most selective 2a blocker we have ??, posted by linkadge on January 13, 2005, at 16:48:07
> I just want something to augment my zoloft without it having too much extra effect.
>
>
> I know selective is a relative term but, some have more affinity for the 2a receptors than other systems they affect.
>
> LinkadgeTodd gave an excellent synopsis. Risperidone sounds like it's worth a trial. You could titrate up from a very low dose (.25 mg?).
Lar
Posted by banga on January 13, 2005, at 22:21:59
In reply to Re: what is most selective 2a blocker we have ?? » linkadge, posted by Larry Hoover on January 13, 2005, at 17:45:13
That's why I think Geodon and Risperdal both helped me with anxiety. Those darn side effects though....clomipramine also hit the target. My theory is that's what helps my anxiety the most.
Posted by SLS on January 14, 2005, at 3:07:29
In reply to Re: what is most selective 2a blocker we have ??, posted by banga on January 13, 2005, at 22:21:59
> That's why I think Geodon and Risperdal both helped me with anxiety. Those darn side effects though....clomipramine also hit the target. My theory is that's what helps my anxiety the most.
Sounds good to me. I wish you continued success with these drugs.
By the way, have you ever tried Remeron or Serzone?
- Scott
Posted by banga on January 14, 2005, at 9:54:54
In reply to Re: what is most selective 2a blocker we have ?? » banga, posted by SLS on January 14, 2005, at 3:07:29
Unfortunately, as I posted on some other threads just this morn, Geodon poops out in two months, and clomipramine seems to have, though now I am not so sure.
I tried Remeron, but then again I was using alcohol heavily at the time so I shouldnt even see it as a trial. I am a little leery of weight gain--my back goes out if I gain even a little weight. I just tried nortryptiline, gained weight dramatically fast--and boom my back was on the verge of going out on me.
I tried Serzone and hated it. Felt drunk.
So all that have the 5HT-2a help but I can't understand if it is only short-term or what.
Posted by SLS on January 14, 2005, at 11:34:45
In reply to Re: what is most selective 2a blocker we have ?? » SLS, posted by banga on January 14, 2005, at 9:54:54
I hope someone here is able to come up with an alternative. I imagine Nardil will be mentioned at some point. Maybe even Buspar. Buspar is a funny drug. When it works, it works well, but it takes at least 2 weeks to see a result. It is like standard antidepressants in that regard.
GOOD LUCK!!!
- Scott
> Unfortunately, as I posted on some other threads just this morn, Geodon poops out in two months, and clomipramine seems to have, though now I am not so sure.
> I tried Remeron, but then again I was using alcohol heavily at the time so I shouldnt even see it as a trial. I am a little leery of weight gain--my back goes out if I gain even a little weight. I just tried nortryptiline, gained weight dramatically fast--and boom my back was on the verge of going out on me.
> I tried Serzone and hated it. Felt drunk.
> So all that have the 5HT-2a help but I can't understand if it is only short-term or what.
Posted by banga on January 14, 2005, at 12:09:39
In reply to Re: what is most selective 2a blocker we have ?? » banga, posted by SLS on January 14, 2005, at 11:34:45
Well I see my pdoc in 2 hours, I wrote down what I would like to discuss, including MAOIs. Or possibly desipramine for the depression, and something else for anxiety--maybe she'll agree to a trial of klonopin? though I am not evensure I want it.....
But clomipramine (and in my estimation its 5ht2a antagonism) was awesome when it worked. My husband keeps bugging me "WHY are you not on Anafranil??" because he noted my response when it did work.
Posted by linkadge on January 14, 2005, at 15:40:14
In reply to Re: what is most selective 2a blocker we have ?? » SLS, posted by banga on January 14, 2005, at 12:09:39
I think anafranil is my first order of buisness since celexa + periactin was probably the best combination for me.
Zoloft is making me very paranoid. I think the depakote helps but only at low doses.
I am getting this horrible "phase out problem" where I suddenly slip into this "bliss" mode where I feel everywhere at once.
I also have these horrible sensations where it feels like my head is being pulled this way and that by giant invisable magnets.
I am a little bit leary of anafranil's anticholinergic side effects since I am a student.
I am not feeling like myself though folks, pray for me.
Linkadge
Posted by ed_uk on January 14, 2005, at 16:03:58
In reply to Re: what is most selective 2a blocker we have ??, posted by linkadge on January 14, 2005, at 15:40:14
Link,
>I am not feeling like myself though folks, pray for me.
We all wish you the best :-)
Do you think you'll try Anafranil? I was unsure why you didn't seem keen on the idea of Lamictal.
Ed.
Posted by linkadge on January 14, 2005, at 17:33:00
In reply to Re: what is most selective 2a blocker we have ?? » linkadge, posted by ed_uk on January 14, 2005, at 16:03:58
I could try lamictal, but I'm just not convinced that it could be so great.
Linkadge
Posted by banga on January 14, 2005, at 18:46:20
In reply to Re: what is most selective 2a blocker we have ??, posted by linkadge on January 14, 2005, at 17:33:00
I'm the Anafranil cheerleader, so my point of view is definitely very subjective. I had NO side effects other than some weight gain, I was happy and clear-headed and positive; but of course others have bad experiences with it...
With 200 mg lamictal (2months on Lamictal together) , I feel it to be fairly benign--it does seem to rid me of those sudden drops into painful despair. No signs of a rash for me at any point. But I doubt it will do the trick alone.....
Just thought I'd drop that quite uninsightful self-observation since I was in the neighborhood and have taken both meds.
Posted by linkadge on January 14, 2005, at 19:03:59
In reply to Re: what is most selective 2a blocker we have ?? » linkadge, posted by banga on January 14, 2005, at 18:46:20
You mean the anafranil won't do the trick alone ??
or the lamictal.Linkadge
Posted by jujube on January 16, 2005, at 13:33:41
In reply to Re: what is most selective 2a blocker we have ??, posted by linkadge on January 14, 2005, at 15:40:14
> I am a little bit leary of anafranil's anticholinergic side effects since I am a student.-- I have not experienced any cognitive problems or any daytime sedation in the time that I have been on Anafranil. That being said, I have only been on it for about 2 months, and at a low dose (50 mg). I tried to go up to 75 mg, but found that the dizziness and hypotension I had already been experiencing at 50 mg became more problematic. However, I have low blood pressure, and had already been experiencing hypotension and some dizziness before I went on Anafranil. If I had been able to tolerate a higher dose, I think it would have been a very effective antidepressant.
Good luck to you Linkage, My thoughts are with you. Take good care of yourself.
>
> I am not feeling like myself though folks, pray for me.
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> Linkadge
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Posted by jujube on January 16, 2005, at 13:40:13
In reply to Re: what is most selective 2a blocker we have ?? » SLS, posted by banga on January 14, 2005, at 9:54:54
Banga,
If not for the weight gain, did you find nortriptyline an effective antidepressant, particularly for anhedonic depression? Did you find it exacerbated your anxiety in any way? Finally, did you find it pro-social?
Sorry for all the questions. Anything you can tell me would be appreciated.
Thanks.
> Unfortunately, as I posted on some other threads just this morn, Geodon poops out in two months, and clomipramine seems to have, though now I am not so sure.
> I tried Remeron, but then again I was using alcohol heavily at the time so I shouldnt even see it as a trial. I am a little leery of weight gain--my back goes out if I gain even a little weight. I just tried nortryptiline, gained weight dramatically fast--and boom my back was on the verge of going out on me.
> I tried Serzone and hated it. Felt drunk.
> So all that have the 5HT-2a help but I can't understand if it is only short-term or what.
Posted by banga on January 16, 2005, at 16:00:55
In reply to ? for Banga » banga, posted by jujube on January 16, 2005, at 13:40:13
I really can't give much help in giving info on Nortryptiline. I did not give it a good trial at all-perhaps 6 days, if even. It was right before New Years, and not to be vain :) but my dress wouldnt even fit anymore, and aside from backaches from the weight gain, I didn't want to go out in public after being absent for a while and be in some old dress and look all puffy.
But I definitely did not feel any other adverse effect either.
Posted by jujube on January 16, 2005, at 20:37:32
In reply to Re: ? for Banga, posted by banga on January 16, 2005, at 16:00:55
Thanks anyway Banga. I appreciate your taking the time to respond.
> I really can't give much help in giving info on Nortryptiline. I did not give it a good trial at all-perhaps 6 days, if even. It was right before New Years, and not to be vain :) but my dress wouldnt even fit anymore, and aside from backaches from the weight gain, I didn't want to go out in public after being absent for a while and be in some old dress and look all puffy.
> But I definitely did not feel any other adverse effect either.
This is the end of the thread.
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