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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 17 of 17. This is the beginning of the thread.
Posted by linkadge on March 23, 2006, at 13:06:30
What is the likelyhood of buspar causing dopaminergically related side effects from d2 antagonism, what is its affinity for these receptors ?
Linkadge
Posted by Meri-Tuuli on March 23, 2006, at 14:01:25
In reply to what is buspar's affinity for d2 ?, posted by linkadge on March 23, 2006, at 13:06:30
Personally, I have no idea, but from SLS's 'drug chart':
"azapirone:
5-HT1a full agonist (pre)
5-HT1a partial agonist (post)
DA2 partial agonist* 1-PP metabolite:
NE-alpha2 antagonist "http://sl.schofield3.home.att.net/medicine/psychiatric_drugs_chart.html
Posted by SLS on March 23, 2006, at 15:02:38
In reply to what is buspar's affinity for d2 ?, posted by linkadge on March 23, 2006, at 13:06:30
> What is the likelyhood of buspar causing dopaminergically related side effects from d2 antagonism,
Are you asking about EPS?
> what is its affinity for these receptors ?You can try this site:
- Scott
Posted by linkadge on March 23, 2006, at 15:07:28
In reply to Re: what is buspar's affinity for d2 ?, posted by SLS on March 23, 2006, at 15:02:38
>Are you asking about EPS?
You have ESP ! :)
Linkadge
Posted by linkadge on March 23, 2006, at 15:10:24
In reply to Re: what is buspar's affinity for d2 ?, posted by SLS on March 23, 2006, at 15:02:38
Yeah, I tried there, couldn't find anything (suprisingly). I was under the impression that it had moderate d2 antagonist properties.
Linkadge
Posted by med_empowered on March 23, 2006, at 15:21:09
In reply to Re: what is buspar's affinity for d2 ?, posted by linkadge on March 23, 2006, at 15:10:24
I dont know..when it first hit the scene, there was hopes that it could be an "atypical antipsychotic," b/c it had some neuroleptic-like effects (ex: taming) in rodents. Didn't pan out. In early studies, they noticed an akathisia-like syndrome (which I experienced @ 45mgs/day). There weren't any cases of TD noted early on, but I seem to recall reading about a couple cases linked to buspirone (no neuroleptics were used in those cases).
Posted by iforgotmypassword on March 23, 2006, at 16:52:06
In reply to buspirone, EPS, D2, posted by med_empowered on March 23, 2006, at 15:21:09
Posted by yxibow on March 23, 2006, at 18:19:55
In reply to what is buspar's affinity for d2 ?, posted by linkadge on March 23, 2006, at 13:06:30
> What is the likelyhood of buspar causing dopaminergically related side effects from d2 antagonism, what is its affinity for these receptors ?
>
> LinkadgeIt has been used experimentally at very high doses for TD treatment, at 3x the highest normal dose, so there is some D2 activity, I haven't found any source that lists a Ki but I imagine the affinity is low unless one has a super high dosage.
Posted by linkadge on March 23, 2006, at 18:21:37
In reply to D2 and alpha2 affinities are prolly comparable? :( (nm), posted by iforgotmypassword on March 23, 2006, at 16:52:06
I think it really sucks that Gepirone was deemed unaprovable. Does this mean that this compound will never see the light of day ?
We lack potent 5-ht1a agonists, despite the fact that SSRI's probably achieve all of their neurotrophic effects through stimulation of 5-ht1a.
Linkadge
Posted by zeugma on March 23, 2006, at 19:15:49
In reply to Gee, its a real shame about Gepirone, posted by linkadge on March 23, 2006, at 18:21:37
i couldn't agree more about the failure of gepirone to be deemed approvable.
of all the drugs in its class buspirone has the lowest parent-to-metabolite ratio, and the highest D2 affinity, thus it is the least desirable member of its class.
Even an ER formulation of buspirone would be useful, but it won't happen. And gepirone is not owned by a company with the clout of, say, Wyeth, whose Effexor metabolite will soon reach the market, and no doubt will prove a valuable advance for those who already respond to Effexor, since the two chemical entities are virtually identical.
-z
Posted by Caedmon on March 23, 2006, at 19:16:51
In reply to what is buspar's affinity for d2 ?, posted by linkadge on March 23, 2006, at 13:06:30
I've been wondering this myself for a long time. I don't think EPS is very common to buspirone however (at least, no more so than SSRIs?).
Can anyone provide a drug-drug comparison? E.g. buspirone's d2 antagonism at 15mg is on par with drug X at dose Y? Or something like that? Even a ballpark figure would be great.
- C
Posted by Phillipa on March 23, 2006, at 21:53:25
In reply to Re: what is buspar's affinity for d2 ?, posted by Meri-Tuuli on March 23, 2006, at 14:01:25
Merri do you understand what link is talking about? I'm really starting to feel stupid. Love Phillipa
Posted by jerrympls on March 24, 2006, at 0:18:45
In reply to Re: what is buspar's affinity for d2 ? » Meri-Tuuli, posted by Phillipa on March 23, 2006, at 21:53:25
Hey-- while we're on the subject of BuSpar - do you think it may help my relentless anxiety/panic/irritability? I've heard it's nothing on it's own - but WITH an AD it's been found useful. I need something to stabliaze me - just a general basic calm. Think it's worth a try?? I've heard mostly negative stuff about it - so someone please give me some good news!
Thanks!!!
Jerry :-)
Posted by yxibow on March 24, 2006, at 1:09:33
In reply to Re: what is buspar's affinity for d2 ? » Meri-Tuuli, posted by Phillipa on March 23, 2006, at 21:53:25
> Merri do you understand what link is talking about? I'm really starting to feel stupid. Love Phillipa
Don't feel stupid -- I only learn by discovery... to fully describe affinity, here's a graduate level example:http://www.mc.uky.edu/Pharmacology/instruction/pha824mp/PHA824mp.html
A particular compound or drug has an affinity for (usually more than one) receptor in the brain. Affinity means how strongly the medication occupies the receptor. These are usually measured in Ki values, the dissociation constant, Kd, the equilibrium constant, and nM, the nanomolar (one mole of molecules has a mass equal to the molecular weight of the compound in grams) and the lower the value, the stronger the drug will occupy a receptor.There is a chart, but it can only be accessed from academic institutions that subscribe to it:
http://www.cpa-apc.org/Publications/Archives/CJP/2002/february/inReviewSeemanPhilipTable1.asp
I'm sure there are others out on the web -- in fact I know there are several powerpoint presentations I forget seeing, I just happened upon this one at the moment.
This study notes that besides Perphenazine (very strong) and Fluphenazine (Prolixin), Haloperidol (Haldol) has among the lowest K (which I believe are averages of Ki and Kd) values (inverse is stronger) -- less than 1.0, which means that they grab onto your D2 receptors like a powerful magnet whereas Quietapine (Seroquel) has a K value of 122 which means it grabs it lightly and lets go.
Then there are values also mentioned in IC50 -- "inhibitory concentration" -- "The molar concentration of an antagonist, which produces 50% of the maximum possible inhibitory response for that antagonist."
(http://www.everythingbio.com/glos/definition.php?word=IC50)It gets quite complicated after here, and goes over my head although I get the general gist of it, having never taken a pharmacology course.
I'm sure someone else can jump in.
Tidings
- J
Posted by Tony P on March 24, 2006, at 1:47:34
In reply to Re: what is buspar's affinity for d2 ?, posted by jerrympls on March 24, 2006, at 0:18:45
> Hey-- while we're on the subject of BuSpar - do you think it may help my relentless anxiety/panic/irritability? I've heard it's nothing on it's own - but WITH an AD it's been found useful. I need something to stabliaze me - just a general basic calm. Think it's worth a try?? I've heard mostly negative stuff about it - so someone please give me some good news!
>
> Thanks!!!
> Jerry :-)Here's my good-news story:
I was once briefly on Buspar by itself while withdrawing from benzos -- it didn't help the withdrawal, but I remembered the experience of increased energy and less stress later.
Subsequently, I was tentatively diagnosed with depression. After a negative experience with Paxil, I went on Serzone and got immediate relief of my sleep disorders and some anti-depressant benefit. After several months of feeling some energy was missing from my emotional life and that I was reacting to stress with anger and depression, I recalled the Buspar experience and suggested it to my Dr. We tried it in combination with the Serzone, and the result was almost magical. I could sleep, I wasn't depressed, I had plenty of energy, and I was able to feel feelings I had suppressed for years.
Re the irritability -- the thing that stood out for me was that with the Buspar when I came home from work I no longer automatically blew up at the kids. I also had less social anxiety and better self-esteem; the effect was subtle but definite.
At the time, Buspar was not commonly known as an AD adjuvant, but I had some correspondence with one other person (it might have been in the early days of this board) who had the same positive experience with the Serzone/Buspar combo.
Alas, the Serzone pooped out about the same time it was taken off the market in Canada, and the Lamictal I have been on the past two years seemed to suppress the effect of the Buspar, so I stopped taking the latter. I am now going off the Lamictal as a trial so I may ask to start the Buspar again.
I consider buspirone absolutely worth a try -- it has very few side-effects, so it will either help you or do nothing. Make sure you try a sufficient dose for a fair trial -- I started at 20 mg/day and was later able to cut back, but many people benefit from a higher dose.
Tony
Posted by Meri-Tuuli on March 24, 2006, at 8:08:18
In reply to Re: what is buspar's affinity for d2 ? » Meri-Tuuli, posted by Phillipa on March 23, 2006, at 21:53:25
Posted by linkadge on March 24, 2006, at 9:57:02
In reply to Re: what is buspar's affinity for d2 ? » jerrympls, posted by Tony P on March 24, 2006, at 1:47:34
5-ht1a agonists are have been touted "serenics".
If you take an SSRI, and you co-administer a 5-ht1a antagonist, you automatically eliminate the antidepressant and anxioloitic properties. In addition you eliminate the neurotrophic effects of the SSRI.
A lot of medicinal herbs, like dong quai, and black co-hosh, SJW, ginkgo, even marajuanna act as 5-ht1a agonists, and may derive some of their theraputic effects from it.
I think that if we had a really potent, and selective 5-ht1a agonist, we might be able to improve certain aspects of the disorder.
Linkadge
This is the end of the thread.
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