# Did anyone try high doses of buspar?



## crayzyMed (Nov 2, 2006)

Apperantly 5HT1A should be a major anxiolytic, so makes me wonder why buspar doesnt work for most of us. Maybe we need to take higher doses?


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## jer (Jun 16, 2009)

I've tried high doses. it didnt work.

doctors like it because it has least side effects.

It does work for a few people and if it does, then that is the best medication.


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## crayzyMed (Nov 2, 2006)

jer said:


> I've tried high doses. it didnt work.
> 
> doctors like it because it has least side effects.
> 
> It does work for a few people and if it does, then that is the best medication.


Well, is anyone up for 1200mg?
Beleive me or not it was used in that dose in a trial...


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## euphoria (Jan 21, 2009)

Buspirone (either directly or through its active metabolite) has D2 and α2-blocking effects, in addition to those on the 5-HT1A receptor. These things are probably what make buspirone such a weak anxiolytic and antidepressant, and the receptor profile (or ratio of effects, shall we say) isn't going to change with higher dosage.

Consider that clonidine (an α2 agonist) is used for performance anxiety, opiate withdrawal anxiety, etc. -- the opposite effect is not something you'd seek out for anxiety disorders, but maybe for depression. The D2 receptor is very important for our experience of pleasure, and blocking it (as buspirone / its metabolite does) promotes anhedonia, depression and antipsychotic effects. Even if buspirone's interaction with those receptors is weak, it's not clinically irrelevant.

Really I think buspirone was a flawed drug from the outset, but it obviously works for some people. If I were you, I wouldn't bother megadosing it because the effect on "undesirable receptors" will increase, but maybe (at normal dosage) buspirone could be considered as an augmentation strategy (e.g. with an SSRI). Personally I am waiting for better meds to target 5-HT1A; they are in development.


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## TiMeZuP (Sep 30, 2009)

euphoria said:


> Personally I am waiting for better meds to target 5-HT1A; they are in development.


How would a med targeting 5-HT1A receptor help us with pleasure from dopamine? Isn't the 5-HT1A receptor related to to Serotonin? What meds are in development, can you list your source......

Thanks......


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## euphoria (Jan 21, 2009)

TiMeZuP said:


> How would a med targeting 5-HT1A receptor help us with pleasure from dopamine? Isn't the 5-HT1A receptor related to to Serotonin? What meds are in development, can you list your source......
> 
> Thanks......


The brain is a very complicated thing, I don't think it could be reduced to that level of simplicity. Imagine (theoretically) something called "neurotransmitter X", it may affect multiple types of receptors in varying locations of the brain, some could increase "neurotransmitter Y" levels, some could decrease them.

The 5-HT1A receptor is a serotonin (5-HT) receptor, and to answer your question, "5-HT1A receptor activation has been shown to increase dopamine release in the medial prefrontal cortex, striatum, and hippocampus" (just from Wikipedia, I know not a source but w/e).

BTW, I was talking about the 5-HT1A agonists listed on here:

http://www.neurotransmitter.net/newdrugs.html

In Japan they already have one in use AFAIK, called tandospirone.

So yeah, I think serotonin receptors are a hugely important target if you have a mood disorder, even if current methods of doing so are still relatively unsophisticated & clumsy.


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## crayzyMed (Nov 2, 2006)

Does this one look better?

Urapidil is a sympatholytic antihypertensive drug. It functions as an α1-adrenergic receptor antagonist, α2-adrenergic receptor agonist, and 5-HT1A receptor agonist.[1] Urapidil is currently not approved by the U.S. Food and Drug Administration, but it is available in Europe.


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## jim_morrison (Aug 17, 2008)

Buspar seems pretty useless, if you really want to blast your 5HT1A receptor, it would make more sence to take an SRI + mirtazapine to block the other 5HT receptors to redirect and simultaneously release more SERT at 5HT1A.


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## crayzyMed (Nov 2, 2006)

A combo with pindolol would be interesting..


> Selective activation of postsynaptic 5-HT1A
> receptors induces rapid antidepressant response
> by
> Blier P; Bergeron R; de Montigny C
> ...


Apperantly buspar is flawed because it also activates the 5HT1A autoreceptors wich has an opposite effect then the normal 5HT1A receptors.

An effexor, remeron, agomelatine, buspar, pindolol combo should be very effective, maybe a few treatment resistans could try it...
Serotonin rocketfuel 10000++
I would watch out for serotonin syndrome tough.


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## crayzyMed (Nov 2, 2006)

euphoria said:


> The brain is a very complicated thing, I don't think it could be reduced to that level of simplicity. Imagine (theoretically) something called "neurotransmitter X", it may affect multiple types of receptors in varying locations of the brain, some could increase "neurotransmitter Y" levels, some could decrease them.
> 
> The 5-HT1A receptor is a serotonin (5-HT) receptor, and to answer your question, "5-HT1A receptor activation has been shown to increase dopamine release in the medial prefrontal cortex, striatum, and hippocampus" (just from Wikipedia, I know not a source but w/e).
> 
> ...


If i could tell it would cure me i would fly to japan to get tandospirone lol:b


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## planetmed (Oct 26, 2010)

Just want to say HI to everyone! 
The last weeks and months i only read posts from you guys which really helped me with my SAD and Depression! In past i took meds from doctors but now i want to know what i'm taking and if there is something better 

1st sorry for my english smile and now here is my 1st post regarding buspar and 5HT1A.

I am interested in Buspar as treatment for sexual disfunction with SSRI. I am taking currently Celaxa but want to switch to Lexapro.
What i understood right know, Sexual Dysfunction is caused from SSRI by acting on 5HT2 Receptors. Though acting on 5HT1A like Buspar which is a 5HT1a Agonist is fine for anxiety and libido, thats why it is used from some together with an SSRI to avoid sexual dysfunction. But Buspar has the disadvantage acting as a (weak) D2 Antagonist.

I found out Trazdodone is an 5HT1A Agonist (better than buspar) AND blocks 5HT2 AND is no D2 Antagonist!

http://jop.sagepub.com/content/19/3/235.abstract

http://www.holisticonline.com/remedies/depression/dep_antidepressant-serotonin-antagonists.htm

So, is Trazodone even better than Buspar for Anxiety and Sexual Dysfunction with SSRI and don't need Buspar?

But you must know Trazodone acts on 5HT1a only from 150mg above doses. Below it is only a sleep aid. 150mg will completely knock you out, so you have to take it at night. But for people with sleeping problems like me it could be the perfect med.
I started at 50mg, noticed a tolerance and currently i am taking 150mg. Think about it to go a little bit higher soon.


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## crayzyMed (Nov 2, 2006)

The problem with trazadone is that the 5HT1A agonism will occur at night leaving you without benefits when you wake up (its half life is short).

Besides that 5HT2A antagonism is a bad thing since 5HT2A plays a crucial role in dopamine release, and dopamine is something very important for us since its highly implicated in social behavor.

Read this post on trazodone for more information:
http://www.socialanxietysupport.com/forum/1318943-post2.html


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## Comfortably Glum (Jan 6, 2010)

What about Tianeptine (selective serotonin reuptake enhancer) on top of Buspar?
Would there be a possible synergistic effect?


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## crayzyMed (Nov 2, 2006)

Comfortably Glum said:


> What about Tianeptine (selective serotonin reuptake enhancer) on top of Buspar?
> Would there be a possible synergistic effect?


It has zero effiacy in social anxiety, only some effectiveness in GAD, for more info read this thread:
http://www.mindandmuscle.net/forum/index.php?showtopic=41412&view=findpost&p=590634

If you dont have GAD i wouldnt bother with buspar.


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## Comfortably Glum (Jan 6, 2010)

I gave buspar a shot earlier this year at 15mg twice a day. 
At around the third week I definitely seemed to have a little more pep in my step. Mornings seemed to feel much more brighter.

Generally I don't suffer from any type of depression, so being extra motivated was a pleasant surprise. Even my gf took notice to how optimistic i had become.

It's hard to say whether there was any effect on my GAD. Since i stopped drinking my GAD was already in decline.
There was no noticeable effects on my social anxiety.

Now here's where buspar *really* shines. 
I already have a pretty healthy sex drive; have to "clean the pipes" maybe 4-5 times a week. However while on buspar i was reaching 2-3 times per day Only took frackin commercial with a cute blonde to set me off!
Definitely out of control but i loved every minute of it:b


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## crayzyMed (Nov 2, 2006)

Comfortably Glum said:


> Now here's where buspar *really* shines.
> I already have a pretty healthy sex drive; have to "clean the pipes" maybe 4-5 times a week. However while on buspar i was reaching 2-3 times per day Only took frackin commercial with a cute blonde to set me off!
> Definitely out of control but i loved every minute of it:b


LMAO, so its good for something afterall!


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## rodzer202 (Nov 28, 2010)

*Buspar*

If you are looking for Buspar online visit

http://www.d-drugs.com/?k=Buspar

Informations, side effects and much more.


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## Himi Jendrix (Mar 24, 2010)

Ive tried fairly high dosage of 40+ mg. All it did was give me the brain shivers. It was really uncomfortable and everytime I tried to move my head it would send electrical shock sensations through my body. 

I been taking buspar for around 3 weeks now and I dont think its any good. I dont have GAD, my main deal is SA and agoraphobia.


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## metamorphosis (Dec 18, 2008)

I just started on ganbapentin . 60 mg a day diveded due to a short half life. I'm only on day 4, so I'm not feeling it yet. But no side effects have popped up so thats a good sign. It's known to be a very tolerated drug!


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## crayzyMed (Nov 2, 2006)

Buspar can only be usefull in combination with SSRI's or for GAD.


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## Canadian4Life (Sep 27, 2010)

Tried buspar in high doses it does nothing. Lithium enhances 5-ht1a receptor transmission and can also raise oxytocin levels significantly. It's used (barely anymore) for bipolar but in lower doses 300mg-600mg it does have a very anti-anxiety effect.


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## Ettan (May 30, 2011)

Could Buspirone help with Post-SSRI sexual dysfuction? It's 4 weeks since I discontinued Fluoxetine, and side effects still remains. Or, are there better alternatives for resensitizing the 5-HT1A receptor?


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## Noca (Jun 24, 2005)

crayzyMed said:


> Buspar can only be usefull in combination with SSRI's or for GAD.


Heh that's what I've been telling ppl for years


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## crayzyMed (Nov 2, 2006)

Ettan said:


> Could Buspirone help with Post-SSRI sexual dysfuction? It's 4 weeks since I discontinued Fluoxetine, and side effects still remains. Or, are there better alternatives for resensitizing the 5-HT1A receptor?


Memantine upregulates 5HT1A


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## Ettan (May 30, 2011)

crayzyMed said:


> Memantine upregulates 5HT1A


Ok, thanks. But I don't think my psychiatrist is willing to prescribe an Alzheimer's medication for my PSSD, in which he dosen't beleive exists in the first place, it's all in my head he says.


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## Bacon (Jul 4, 2010)

Iv Heard Of Buspar and i heard its terrible! Doctor's love it because its not a controlled substance.


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## crayzyMed (Nov 2, 2006)

Bacon said:


> Iv Heard Of Buspar and i heard its terrible! Doctor's love it because its not a controlled substance.


Beleive it or not, for GAD its as effective as benzo's, its COMPLETELY useless for all other disorders tough.


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## Arisa1536 (Dec 8, 2009)

Its very ineffective but maybe thats because It gave me headache, lethargy and hunger pangs but made me more depressive too
So if it is as effective as a benzo for GAD it did a wonderful job of disguising the fact :no
Useless in a word

and i took it with SNRI medication


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## Rodney mullin (Oct 24, 2011)

Very strange, I seem to partake in a high from the substance from a mere 10mg. Then again I am mildly schizophrenic, mabye that triggers something or allows the chemicals to affect me slightly different. Anyhow I just crushed up a single pill and snorted it, the moment it whent in my nose my mood had already altered. The euphoria was most un-definable besides nearly every 5-10 seconds it felt like a whole wad of electricity flowed out of my brain and into my body at once only allowing me to feel the current of its flow and nothing else. This continued for a good 15 minutes (I think)


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## crayzyMed (Nov 2, 2006)

Rodney mullin said:


> Very strange, I seem to partake in a high from the substance from a mere 10mg. Then again I am mildly schizophrenic, mabye that triggers something or allows the chemicals to affect me slightly different. Anyhow I just crushed up a single pill and snorted it, the moment it whent in my nose my mood had already altered. The euphoria was most un-definable besides nearly every 5-10 seconds it felt like a whole wad of electricity flowed out of my brain and into my body at once only allowing me to feel the current of its flow and nothing else. This continued for a good 15 minutes (I think)


Buspar is effective for shizophrenia in atleast one trial.


> J Clin Psychopharmacol. 2010 Dec;30(6):678-82.
> A double-blind, randomized, and placebo-controlled trial of buspirone added to risperidone in patients with chronic schizophrenia.
> Ghaleiha A, Noorbala AA, Farnaghi F, Hajiazim M, Akhondzadeh S.
> Source
> ...





> Hum Psychopharmacol. 2009 Aug;24(6):437-46.
> Treatment of cognitive dysfunction in chronic schizophrenia by augmentation of atypical antipsychotics with buspirone, a partial 5-HT(1A) receptor agonist.
> Piskulić D, Olver JS, Maruff P, Norman TR.
> Source
> ...


In this thread i posted a full overview of substances effective for shizophrenia:
http://www.mindandmuscle.net/forum/...cs/40114-post-up-schizophrenic-regimen-6.html


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## DK3 (Sep 21, 2011)

crayzyMed said:


> Apperantly 5HT1A should be a major anxiolytic, so makes me wonder why buspar doesnt work for most of us. Maybe we need to take higher doses?


It works for me but I found the effects take a while to develop when you first start using it (about 4-6 weeks) somewhat like an SSRI. Many take it expecting to get an instant benzo-style effect so think it doesn't work. Also unlike a benzo the effects are more subtle and there's no sedation.

The problem with taking high doses of it is I think it might heighten the "brain zaps" phenomena many report on Buspar. I found even at low-moderate dose of 10mg they are quite prominent when you first begin taking it for the first few weeks.


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## DK3 (Sep 21, 2011)

Rodney mullin said:


> Very strange, I seem to partake in a high from the substance from a mere 10mg. Then again I am mildly schizophrenic, mabye that triggers something or allows the chemicals to affect me slightly different. Anyhow I just crushed up a single pill and snorted it, the moment it whent in my nose my mood had already altered. The euphoria was most un-definable besides nearly every 5-10 seconds it felt like a whole wad of electricity flowed out of my brain and into my body at once only allowing me to feel the current of its flow and nothing else. This continued for a good 15 minutes (I think)


That's very interesting. I've never heard of anyone snorting buspar before! The electricity flows you describe seem to be related to the tiny "brain zaps" many report on Buspar that occur every 20 seconds or so and often just by turning your head or moving. I don't know what causes that exactly but I guess it could be considered a short-term side effect as it generally goes away (or doesn't happen at all) if you lower the dose and take a higher dose incremented more gradually.

When I began taking it at 10mg I didn't feel any euphoria as such, but I did experience the brain zaps which were not unpleasant and interesting to say the least. I also felt "different" and like my brain had shifted to a different level..hard to put into words.. you know like when you're tired or just woke up? Sort of like that, but without any actual tiredness/sedation.


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## crayzyMed (Nov 2, 2006)

For GAD buspar is just as effective as benzo's, i'm no longer a proponent of high doses but i do support its use for GAD, some individuals may also like it for other disorders but the evidence for that is lacking and there are many negative reports.


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## InterestinglyInteresting (May 7, 2010)

Ettan said:


> Could Buspirone help with Post-SSRI sexual dysfuction? It's 4 weeks since I discontinued Fluoxetine, and side effects still remains. Or, are there better alternatives for resensitizing the 5-HT1A receptor?


i dont mean to hijack the thread but may i ask what symptoms of PSSD you have? also fluoxetine has a loooong half life meaning over 2 weeks to at least completely rid your system if i believe.

onto the main topic i havent tried buspar but am reluctant due to its comparable effectiveness to a placebo


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## crayzyMed (Nov 2, 2006)

InterestinglyInteresting said:


> onto the main topic i havent tried buspar but am reluctant due to its comparable effectiveness to a placebo


For GAD its as effective as benzo's, also combined with SSRI's it will be differend and potentiate the antidepressant effects.


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