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Thread: Gabapentin & (Clonazepam, Xanax, Ativan etc)

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    Gabapentin & (Clonazepam, Xanax, Ativan etc) 
    #1
    I'm wondering if someone could explain to me the interaction of gabapentin and typical benzo's (clonazepam, xanax, ativan, etc).

    How do they not contactdict each other, and cancel them out?

    They are all gabatropic drugs. Does taking gabapentin before benzo's, block the effect of the benzo's? Like wise the reverse, can't seem to figure it out
    Last edited by JamtasticX; 11-06-2010 at 03:47. Reason: Like wise the reverse, can't seem to figure it out
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    #2
    Bluelighter Unbreakable's Avatar
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    Neurontin (Gabapentin) is also very closely related to Lyrica (Pregabalin).... Which is a GABA analogue...


    While Clonazepam, Xanax, Ativan are from the benzodiazepine family....

    Hope that helps....
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    #3
    Bluelighter /navarone/'s Avatar
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    I would be really surprised if they really canceled each other reciprocally though I could deduce that somehow they compete at the same receptor eve if not at the same receptor site.



    As the picture above shows, Benzodiazepines target a different area on the GABA-A receptor while a GABA analogue would mostly target the same sites as GABA.
    Probably the conformational change of the protein subunits from the action og gabapentin (wich is indeed much bulkier than GABA) impedes the bonding of benzodiazepines.

    I would find it pretty hard to believe that the activity of the chloride ion channel remains unhibited after the interaction of both Gabapentin and Benzodiazepines.
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    #4
    Quote Originally Posted by /navarone/ View Post
    I would be really surprised if they really canceled each other reciprocally though I could deduce that somehow they compete at the same receptor eve if not at the same receptor site.



    As the picture above shows, Benzodiazepines target a different area on the GABA-A receptor while a GABA analogue would mostly target the same sites as GABA.
    Probably the conformational change of the protein subunits from the action og gabapentin (wich is indeed much bulkier than GABA) impedes the bonding of benzodiazepines.

    I would find it pretty hard to believe that the activity of the chloride ion channel remains unhibited after the interaction of both Gabapentin and Benzodiazepines.

    Thanks for the help, I'll acrhive this pic for sure, along with the thread.

    How can both gaba and bnz bind to the same receptor thought?
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    #5
    Guys, gabapentin does not bind to any GABA receptor. Nor does pregabalin.

    Quote Originally Posted by JamtasticX View Post
    How can both gaba and bnz bind to the same receptor thought?
    Picture them as helicopters landing on the roof of the Pentagon. That thing up there is roughly 300 kilodaltons in mass (almost 3,000 times the mass of the GABA molecule).
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    #6
    Bluelighter dread's Avatar
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    Pregabalin & gabapentin bind to calcium channels.

    this from wikipedia:

    Pregabalin increases neuronal GABA levels by producing a dose-dependent increase in glutamic acid decarboxylase activity.[1] Glutamic acid decarboxylase (GAD) is the enzyme that converts the excitatory neurotransmitter glutamate into the inhibitory GABA in a single step. For this reason, pregabalin greatly potentiates benzodiazepines, barbiturates & other depressants.
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    #7
    Bluelighter Unbreakable's Avatar
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    My friend is prescribed both... Valium & Gabapentin to take daily by a good doctor....so i doubt they would equal each other out... I have personally taken both before i was faced....
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    #8
    Quote Originally Posted by JamtasticX View Post
    Thanks for the help, I'll acrhive this pic for sure, along with the thread.

    How can both gaba and bnz bind to the same receptor thought?

    I wouldn't in reference to gabapentin, pregabalin!

    As mentioned above pregabalin and gabapentin act on calcium channel receptors, if they DIRECTLY act upon GABA receptors it is yet to be discovered! I'm guessing the manufacturers would have looked quite thoroughly in to that. (although might know more than we know)

    ...and no gabapentin does not cancel benzodiazepines out. They merely interact in a sense of INCREASED SEDATION. Gabapentin and pregabalin have very few drug interactions as they mode of action is so different. There are many patients on the combination.
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    #9
    This pharmacology is mostly over my head, but from person experience benzo's are not canceled out by gabapentin. If anything they seem potentiated.
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    #10
    Bluelighter /navarone/'s Avatar
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    If Gabapentin is a calcium channel blocker...then how come that carbamazepine and oxcarbazepine aren't truly psychoactive?
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    #11
    Quote Originally Posted by /navarone/ View Post
    If Gabapentin is a calcium channel blocker...then how come that carbamazepine and oxcarbazepine aren't truly psychoactive?
    Definition of psychoactive:
    A psychoactive drug, psychopharmaceutical or psychotropic is a chemical substance that crosses the blood-brain barrier [Yes to both ox + carb] and acts primarily upon the central nervous system where it alters brain function [yes to ox and carb], resulting in changes in perception, mood, consciousness, cognition, and behavior[both are used in mood disorders + bipolar, also have cns side effects].
    so yes they are psychoactive, fact.

    ..if however you really mean are "fun" or you get any kind of general "high" feeling, that is simply due to pharmacology + completely different structures. Also to note oxcarbazepine + carbamazepine are sodium channel blockers. Whilst Gabapentin and Pregabalin act via the voltage gated N type calcium channels. Don't get confused though calcium channel blocking does not equate to fun, nimodipine (cns calcium channel blocker) is used for subarachnoid haemorrhage and is neither here nor there. Long story short CNS drugs are complicated and unless you are willing to delve in to the nitty gritty dont expect straight forward answers - that however is the fun of ADD here on bluelight!
    Last edited by Phener; 17-06-2010 at 00:39.
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    #12
    I take carbamazepine for nerve pain and some people reported some weird issues. Being sleepy, longer thought processes, etc.

    I never noticed any. I wanted to try oxcarbazepine but until my insurance goes into effect next month, it's cost prohibitve.
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    #13
    My post is 6 months later, but just yesterday SWIM was rx'd 300 mg Gabapentin (generic Neurontin) twice a day to help SWIM's rx'd Ativan "potentiate"/work better. SWIM is rx'd 2mg of Ativan twice a day. SWIM has quite a high tolerance to benzos, has been taking them everyday for 3 and 1/2 years, and he was once taking 10 mgs of Xanax per day. SWIM's doctor knows this and SWIM finds even 2 mg of Ativan often ineffective for agoraphobia and anxiety, so SWIM would sometimes take 3 or 4 mgs at once in order to leave the house. SWIM's doctor is aware of this as well. SWIM nor his doctor want to go back on the path of escalating benzo dosages, so this is why SWIM's doctor rx'd the Gabapentin.

    SWIM took the Gabapentin by itself yesterday and noticed nothing at 300 mg. SWIM looked up dosages and realized 300 was a pretty low dose. SWIM took a total of 600 mg and felt very out of it and disconnected. That was SWIM's only report.

    Today SWIM took 2 mgs of Ativan with 300 mgs of Gabapentin about 30 minutes ago. Will let you know what SWIM says regarding the effects.
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    #14
    Newbie here, sorry. The main point I wanted to make was that SWIM's psychiatrist specifically prescribed the Gabapentin to make the Ativan work better. I assume it would do the same for any benzo. And again, SWIM will make a report to see if this is true or not, at least in his case.
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    #15
    Bluelighter DJHENRU's Avatar
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    Shouldnt swim here. especially about low dose gabapentin and ativan wtf .
    Of couse they potentiate each other, and other things like valarian/California poppys/kava kava, possibly periwinkle or piracetam etc.
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    #16
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    cant read swims properly, please stop it.

    the primary reason i have an interest in gabapentin is to make my zopiclone go further
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    #17
    I was answering a question for JamtasticX. Didn't know about the swim problem on here.
    At any rate, it's been 2 hours and the Ativan and Gabapentin left a more light-headed feeling than the Ativan alone. Not sure how much it potentiates benzos at such a low dose of Gabapentin.
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    #18
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    Quote Originally Posted by banana101 View Post
    I was answering a question for JamtasticX. Didn't know about the swim problem on here.
    At any rate, it's been 2 hours and the Ativan and Gabapentin left a more light-headed feeling than the Ativan alone. Not sure how much it potentiates benzos at such a low dose of Gabapentin.
    because it increases the amount of gaba floating around (by converting glutamate to gaba due to an increase in enzyme activity), and ativan allows gaba to bind to the bzd recpetor more easily. therefore synergy
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    #19
    Bluelighter DJHENRU's Avatar
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    Today I had to awake early, so yeasterday I took a few grams with many grams of valarian, layed so pleasantly with eyes closed for a while and awoke so refreshed.
    absolutely no hangover or rebound so far
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    #20
    when im withdrawling from lyrica or gaba benzos dont work wut so ever
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    #21
    Bluelighter
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    nuke you are the man son. I feel like I'm dying, 16 hours, 2 years, now with pregablin! life is complete! always the best preductive days then hit the pipe and JAM, all that staggered dosing hits like a ton of bricks. can I go to far? really? gabapentin? no way. turned the bathroom light on and saw red light, I mean +3 wtf is happening but only for 30 seconds, eyes fully opened, the most bloodshot I have seen them. the true stimulant, psychedelic and tranquilizer feeling (but somehow slightly euphoric unlike ANY other "knock you out" drug). and this could go on and on.

    DAMN just had to get something out. my question is this: why do some people have such different reactions and does it have anything to do with synapses not firing/rebuidling?
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    #22
    when i was addicted to gaba and pregablin(lyrcica) benzos made my symtoms a million times worse be warey!
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