# Need your gaba sensitivity back?



## Canadian4Life (Sep 27, 2010)

I have been on wellbutrin (bupropion) for a few days now and after all the stories I read on how it causes anxiety I stayed away. I gave it a shot though because nothing was working. I take 2-3mg of clonazepam a day and noticed the second day (of bupropion treatment) that my clonazepam was making me really tired (2mg). I find also since starting wellbutrin I don't feel the need to take my clonazepam at all! I thought i'd need more being on it but I am down to 1mg and feel NO withdrawal. I did some research on wellbutrin (bupropion) and came across a very interesting article.. although it's triazolam not clonazepam in the study I definetly find this to apply to it as well!!

http://content.karger.com/ProdukteDB/produkte.asp?Doi=87189


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## crayzyMed (Nov 2, 2006)

Very interesting, i wonder by what mechanism it does this.


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## martyboi (Sep 18, 2009)

i'm very skeptical. that sounds too good to be true...why don't doctors use bupropion during benzo withdrawal then?


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## crayzyMed (Nov 2, 2006)

martyboi said:


> i'm very skeptical. that sounds too good to be true...why don't doctors use bupropion during benzo withdrawal then?


Because they are ignorant of this, just like they arent aware of NMDA antagonists.


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## martyboi (Sep 18, 2009)

Damn. I'm almost convinced to take up a benzo addiction with the use of dxm and bupropion on my off days. Just for the hell of it.


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## martyboi (Sep 18, 2009)

that was a joke actually. lol....id need more convincing


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## martyboi (Sep 18, 2009)

crayzyMed said:


> Because they are ignorant of this, just like they arent aware of NMDA antagonists.


actually come to think of it....bupropion would almost guarantee a seizure during benzo withdrawal...thats probly why


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## crayzyMed (Nov 2, 2006)

Dude add in topiramate, it protects against seizures and will also help with withdrawal due to its AMPA antagonism, i would think a 3 med approuch would attack a benzo addiction like the sovjet army storming over europe.


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## crayzyMed (Nov 2, 2006)

> Ibogaine is a hallucinogen (psychotomimetic) that some claim interrupts addiction and reduces or eliminates withdrawal syndromes, specifically in regards to opioids.[79] Its mechanism of action is unknown, but likely linked to nAchR α3ß4 antagonism.


Very fascination, looks like some nicotinic receptors play a big role in drug addiction/tolerance/withdrawal.


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## crayzyMed (Nov 2, 2006)

New compounds may treat both alcohol and cigarette addictions


Selena E. Bartlett, PhD

Researchers at the Ernest Gallo Clinic and Research Center at the University of California, San Francisco, and Pfizer Inc., have determined that two new compounds may be effective in treating both alcohol and nicotine dependence at the same time.

In a paper published in the November 3, 2010 issue of Neuropsychopharmacology, the researchers showed that alcohol consumption in rodents was significantly decreased by two compounds that target neuronal nicotinic acetylcholine receptor (nAChR) subtype α3ß4*.

nAChRs are proteins found in the brain and broader central nervous system that mediate the effects of substances such as nicotine. Recent human genetic studies have shown that the genes encoding the α3ß4* subtype are of significant importance for susceptibility to both alcohol and nicotine dependence.

“The problem has been translating these important genetic findings into more effective medications for people,” said co-senior author Selena E. Bartlett, PhD, director of the Preclinical Development group at the Gallo Center. The lead author of the study is Susmita Chatterjee, PhD, of the Gallo Center.

The work was done in collaboration with scientists led by co-senior author Hans Rollema, PhD, in the Neuroscience Research Unit at Pfizer Inc.

One of the new compounds, CP-601932, has been shown in a clinical study to be safe in humans, notes Bartlett. She recommends a clinical study to evaluate the compound’s efficacy and potential benefits in treating both alcohol and nicotine dependence.

The other compound is PF-4575180. Both were developed by Pfizer.

“Alcohol and nicotine addiction are often treated as separate disorders,” Bartlett says, “despite the fact that 60 to 80 percent of heavy drinkers smoke tobacco. There are very few effective strategies for treating these disorders separately, let alone together. Our data suggest that by targeting specific nAChR subtypes, it may be possible to treat both alcohol and nicotine dependence with one medication.”

Significantly, while the compounds had a significant effect on the rodents’ alcohol consumption, their intake of sucrose was not affected. “This indicates that unlike currently approved alcohol abuse medications, the compounds do not interfere with the brain’s natural reward system in a larger way,” says Bartlett.


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## Canadian4Life (Sep 27, 2010)

Bupropion decreases gaba in certain areas of the brain almost like a gaba antagonist and allows them to become sensitive again. Also the upregulation of adrenic receptors and the downregulation bupropion causes maybe a balance and protect against tolerance and reverse gaba and adrenic receptor changes. Using bupropion during benzo withdrawal is a no-no because it raises the seizure threshold which is extremely dangerous in benzo withdrawal. Also the anxiety from benzo withdrawal would sky rocket from bupropion. I'd say in post withdrawal when anxiety has dropped (a month atleast) starting it might be very useful.


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## crayzyMed (Nov 2, 2006)

Canadian4Life said:


> *Bupropion decreases gaba in certain areas of the brain almost like a gaba antagonist and allows them to become sensitive again. *Also the upregulation of adrenic receptors and the downregulation bupropion causes maybe a balance and protect against tolerance and reverse gaba and adrenic receptor changes. Using bupropion during benzo withdrawal is a no-no because it raises the seizure threshold which is extremely dangerous in benzo withdrawal. Also the anxiety from benzo withdrawal would sky rocket from bupropion. I'd say in post withdrawal when anxiety has dropped (a month atleast) starting it might be very useful.


However you were taking a benzo while ON wellbutrin, if it actually caused an antagonistic effect wich would cause upregulation you would have went into withdrawal before any increased sensivity occured, i think this is definatly something because of the α3ß4 antagonism since that receptor is implicated in drug craving, addiction and tolerance.

Agreed that using wellbutrin during withdrawal is a bad idea, i forgot about the seizure thing, but since it appears to reverse tolerance while on them, you can take it this way.

α3ß4 antagonism and GABAB agonism are especially interesting with regards to drug craving.


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## mikoy (Aug 12, 2010)

I think nicotinic receptors are underestimated in depression/anxiety studies.


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## Canadian4Life (Sep 27, 2010)

mikoy said:


> I think nicotinic receptors are underestimated in depression/anxiety studies.


I totally agree with you on that one..in some cases not all


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