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Dr. Bob is Robert Hsiung, MD,
[email protected]Shown: posts 1 to 16 of 16. This is the beginning of the thread.
Posted by Janelle on December 2, 2003, at 16:11:31
I read a thread way above regarding Buspar, which I have been on for over a year. I cannot understand all the technical jargon in that thread -- could someone explain in a simple way what the deal is with antidepressants acting on HT1 receptors (are they an agonist or antagonist) and what receptor(s) Buspar acts on and is it an agonist or an antagonist.
I am now totally confused about how Buspar works! It is anti-anxiety but I get the impression it may also help depression?
Anyone with a concise explanation appreciated.
Posted by shadows721 on December 2, 2003, at 18:46:32
In reply to HELP - BUSPAR, part 2: total confusion!, posted by Janelle on December 2, 2003, at 16:11:31
I don't understand all the chemistry of this med either. I do know that I felt it lift my depression a bit and didn't feel it helped me in the anxiety arena. So, yes, I felt this med acted like a very weak antidepressant in my case. My doc shook his head that this drug is not a weak antidepressant, but it really reacted that way with me. I found that colors really looked a lot brighter. I found that similiarity when I was on prozac. Odd isn't it.
Posted by zeugma on December 2, 2003, at 20:16:35
In reply to Re: HELP - BUSPAR, part 2: total confusion!, posted by shadows721 on December 2, 2003, at 18:46:32
> I don't understand all the chemistry of this med either. I do know that I felt it lift my depression a bit and didn't feel it helped me in the anxiety arena. So, yes, I felt this med acted like a very weak antidepressant in my case. My doc shook his head that this drug is not a weak antidepressant, but it really reacted that way with me. I found that colors really looked a lot brighter. I found that similiarity when I was on prozac. Odd isn't it.
I find Buspar to be nothing like Klonopin (a true anxiolytic!) but it lifts my mood, has a slight calming/sedative effect, and helps me sleep.
Posted by sb417 on December 2, 2003, at 21:54:14
In reply to Re: HELP - BUSPAR, part 2: total confusion!, posted by zeugma on December 2, 2003, at 20:16:35
Zeugma, you said Buspar helps you sleep, so I assume you take it at night, right before bed? How much do you take? Thanks.
Posted by scott-d-o on December 2, 2003, at 22:54:22
In reply to HELP - BUSPAR, part 2: total confusion!, posted by Janelle on December 2, 2003, at 16:11:31
> I read a thread way above regarding Buspar, which I have been on for over a year. I cannot understand all the technical jargon in that thread -- could someone explain in a simple way what the deal is with antidepressants acting on HT1 receptors (are they an agonist or antagonist) and what receptor(s) Buspar acts on and is it an agonist or an antagonist.
>
> I am now totally confused about how Buspar works! It is anti-anxiety but I get the impression it may also help depression?
>
> Anyone with a concise explanation appreciated.Buspirone is a full agonist at 5-HT1a presynaptic autoreceptors, and a partial agonist at postsynaptic 5-HT1a receptors. The autoreceptors are a feedback mechanism for how much 5-HT is in the synapse so this has the overall effect of decreasing serotonin in the synapse. It also has an affinity for dopamine receptors although it is much weaker than the 5-HT1a binding. Here there is some confusion, I have heard that it acts both as an agonist and antagonist at D2 receptors but the general consensus is that it is a antagonist at presynaptic D2 autoreceptors which should increase dopamine in the synapse. I believe people attribute buspirone's antidepressant activity to its metabolite, 1-PP, which is a NE alpha2 antagonist (i.e. yohimbine), which are presynaptic and increase the release of norepinephrine. NE alpha2 antagonists also have pro-sexual effects. This metabolite is actually found in much greater concentrations in the blood after buspirone than the unchanged drug itself. Hope this helps.
Scott
Posted by Janelle on December 3, 2003, at 16:13:12
In reply to Re: HELP - BUSPAR, part 2: total confusion!, posted by scott-d-o on December 2, 2003, at 22:54:22
I sort of followed your explanation of the receptors, etc. My main question is does Buspar affect SEROTONIN (5HTP?) and if so how - does it increase or decrease serotonin??? Thanks.
Posted by zeugma on December 3, 2003, at 17:06:13
In reply to Re: HELP - BUSPAR, part 2: total confusion! » zeugma, posted by sb417 on December 2, 2003, at 21:54:14
> Zeugma, you said Buspar helps you sleep, so I assume you take it at night, right before bed? How much do you take? Thanks.
I take 15 mg in the morning and 15 mg at night. It helps me sleep, but it doesn't put me to sleep, if you know what I mean. (I also take Klonopin in a tiny dose first thing in the morning.) Since Buspar is the only med I take 2x a day, I sometimes forget to take my second dose and find that my insomnia returns. Above 30 mg a day, and i want to sleep around the clock.
Posted by SLS on December 3, 2003, at 20:59:21
In reply to HELP - BUSPAR, part 2: total confusion!, posted by Janelle on December 2, 2003, at 16:11:31
Hi Janelle.
You should be confused. I am too. There is nothing straight foward about serotoninergic neurotransmission.
I don't have much confidence in my own understanding of Buspar. I do know that Buspar (buspirone) was originally developed as an antidepressant, but was approved only for anxiety. Some doctors will use it to augment antidepressants.
I've given up trying to figure out how drugs work.
Buspar is known to do a few things that might or might not be relevant to its clinical profile. From what I remember, it:
1. Acts as a full agonist at presynaptic 5-HT1a receptors
- reduces the synthesis and release of serotonin
? reduces anxiogenic serotoninergic hyperactivity"Schreiber and DeVry (62) hypothesized that the anxiolytic effects of 5-HT1A partial agonists result predominantly from an interaction with presynaptic 5-HT1A receptors, resulting in a decrease of hyperactive serotonergic neurotransmission" - Jeremy D. Coplan, Susan I. Wolk, and Donald F. Klein
2. Acts as a partial agonist at postsynaptic 5-HT1a receptors
- increases or decreases neuronal excitability, depending on location
- inhibits adenylate cyclase and reduces the formation of cAMP second messenger
? reduces postsynaptic desensitization"Based on in vivo electrophysiological experiments, Blier et al. have postulated that 5HT1A partial agonists mediate antidepressant effects through a net increase in serotonergic neurotransmission following adaptive receptor changes." - Jeremy D. Coplan, Susan I. Wolk, and Donald F. Klein
* It should be noted that it takes 2-3 weeks for these adaptive changes to develop, which mirrors the time it takes for Buspar to demonstrate anxiolytic effects. As an augmentor of antidepressants, I don't know how long it takes to see results.
3. Acts as a moderate antagonist at dopamine D2 receptors.
- similar to neuroleptic antipsychotics
? acute sedative effects
This probably was not very helpful. Sorry.
- Scott
Posted by Tony P on December 4, 2003, at 3:48:03
In reply to Re: HELP - BUSPAR, part 2: total confusion!, posted by scott-d-o on December 2, 2003, at 22:54:22
> Scott: [much good info clipped] I believe people attribute buspirone's antidepressant activity to its metabolite, 1-PP, which is a NE alpha2 antagonist (i.e. yohimbine), which are presynaptic and increase the release of norepinephrine. ... This metabolite is actually found in much greater concentrations in the blood after buspirone than the unchanged drug itself. Hope this helps.
>
> ScottThat probably explains why I always get the activating effect about 2 hours _after_ taking Buspar, when the slightly dopey feeling wears off. BTW, I have always had an immediate activating and stress-reducing response to Buspar, although it's a moot point now since I take it regularly (20-30mg/day).
It used to _prevent_ me from sleeping, so I always took it morning & noon, but lately it has made me sleepy if I am lying down in a quiet place. Our bodies just keep on adapting....
Tony
Posted by SLS on December 4, 2003, at 6:54:10
In reply to Re: HELP - BUSPAR, part 2: total confusion!, posted by Tony P on December 4, 2003, at 3:48:03
> Scott: [much good info clipped] I believe people attribute buspirone's antidepressant activity to its metabolite, 1-PP, which is a NE alpha2 antagonist (i.e. yohimbine), which are presynaptic and increase the release of norepinephrine. ...
Thank you! I completely forgot about that!
Unfortunately Remeron and idazoxan worsen my depression, otherwise I probably would have tried Buspar by now. The 1-PP thing happens with gepirone too. For me, that sucks, but for you, perhaps it is a cleaner drug. Gepirone was close to getting approved last I heard. The 5-HT1a agonist that I would like to have seen developed is flesinoxan. It isn't metabilized into 1-PP.
> This metabolite is actually found in much greater concentrations in the blood after buspirone than the unchanged drug itself. That probably explains why I always get the activating effect about 2 hours _after_ taking Buspar, when the slightly dopey feeling wears off.
Do you think the dopey feeling is due to DA D2 blockade? Gepirone is supposed to be free of that.
> BTW, I have always had an immediate activating and stress-reducing response to Buspar, although it's a moot point now since I take it regularly (20-30mg/day).
Hmmm. Maybe I should give it a try at some point - maybe with Effexor.
> It used to _prevent_ me from sleeping, so I always took it morning & noon, but lately it has made me sleepy if I am lying down in a quiet place. Our bodies just keep on adapting....
I wish my body wasn't so adaptive. When once I responded robustly to a combination of Parnate + desipramine, now it is of little help. I have had numerous 3-day responses to antidepressants, only to have my system adapt to them and allow me to relapse.
Thanks for posting.
- Scott
Posted by Gidon on December 7, 2003, at 23:38:53
In reply to Re: HELP - BUSPAR, part 2: total confusion!, posted by scott-d-o on December 2, 2003, at 22:54:22
>NE alpha2 antagonists also have pro-sexual effects.What is the dosage of buspar if I want to exploit that pro-sexual effect? I desperately need something to restore my sexual desire which I lost to zoloft. Please respond
Thanks Scott
GR
Posted by Ilene on December 10, 2003, at 20:41:04
In reply to Re: HELP - BUSPAR, part 2: total confusion!, posted by zeugma on December 3, 2003, at 17:06:13
> I take 15 mg in the morning and 15 mg at night. It helps me sleep, but it doesn't put me to sleep, if you know what I mean. (I also take Klonopin in a tiny dose first thing in the morning.) Since Buspar is the only med I take 2x a day, I sometimes forget to take my second dose and find that my insomnia returns. Above 30 mg a day, and i want to sleep around the clock.
>
>
Is there any interaction between the Klonopin & the BuSpar?Thanks,
Ilene
Posted by zeugma on December 10, 2003, at 22:44:12
In reply to Re: HELP - BUSPAR, part 2: total confusion! » zeugma, posted by Ilene on December 10, 2003, at 20:41:04
> > I take 15 mg in the morning and 15 mg at night. It helps me sleep, but it doesn't put me to sleep, if you know what I mean. (I also take Klonopin in a tiny dose first thing in the morning.) Since Buspar is the only med I take 2x a day, I sometimes forget to take my second dose and find that my insomnia returns. Above 30 mg a day, and i want to sleep around the clock.
> >
> >
> Is there any interaction between the Klonopin & the BuSpar?
>
> Thanks,
>
> IleneI don't know, since i've never taken K by itself. Unintentionally, however, I may receive some insight on this front. My prescription of Buspar is almost out (down to my last 10 mg pill) and due to a combination of circumstances, I will not be able to get a refill until Friday.
I would *guess*, from some hints of what I've read on this board, and from Buspar's general rep as a synergistic drug, that the Buspar gives the K some help in the anxiolysis department. It would be a little ironic if this were true, since I gather that Buspar was once billed as a nonaddicting alternative to the benzodiazepines. I do know for sure that before I added the Klonopin (.25 mg am) I was having anxiety attacks regularly.
z
Posted by Gusto on December 12, 2003, at 15:58:23
In reply to Re: HELP - BUSPAR, part 2: total confusion! » scott-d-o, posted by Gidon on December 7, 2003, at 23:38:53
I take zoloft (was at 50mg, now at 25mg) and had problems with the libido. Since adding buspar back into the mix (30mg) I'm once again my horny old self.
Posted by Jed_9 on December 13, 2003, at 22:13:28
In reply to Re: HELP - BUSPAR, part 2: total confusion!, posted by Gusto on December 12, 2003, at 15:58:23
Anyone with success helping sexual side effects from psych meds please share... With Buspar, Wellbutrin, or other meds. Even how common is it to use Viagra or similiar because of SSRI or antipsychotic sexual dysfunction. I need the feedback please.
Thank you.
Posted by HIBA on December 16, 2003, at 0:45:39
In reply to Re: HELP - BUSPAR, part 3: sexual success stories!, posted by Jed_9 on December 13, 2003, at 22:13:28
Don't be overenthusiastic here. Buspar helped erection at least for a short period. I don't know how it helped but the effect was there. Unfortunately it didn't help with the lack of desire and negatively affected orgasm too. Orgasm on buspar was a pleasureless experience and I left that stuff. Before trying any viagra buspar should be given a chance if the problem is with erectile difficulties. But for the lack of desire, I think a dopaminergic like bromocriptine may help but the good effects soon poop out even after continued dose increases. This is my experience.
HIBA
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